3,4-substituted pyrrolidine derivatives for treating hypertension

FIELD: chemistry.

SUBSTANCE: present invention relates to novel 3,4-substituted pyrrolidine derivatives of general formula or pharmaceutically acceptable salts thereof, where R1 is an acyl selected from values given paragraph 1 of the formula of invention; R2 is unsubstituted C1-C4-alkyl or C3-C7-cycloalkyl; R3 is a fragment selected from a group of fragments of formulae: (a), (b),

(c) and (f), where any of the fragments of formulae given above (a), (b) and (f), the star (*) indicates a bond of the corresponding fragment R3 with the molecule residue in formula I; Ra denotes N-C1-C4-alkylaminocarbonyl, N-phenylaminocarbonyl, N-(phenyl-C1-C4-alkyl)aminocarbonyl, N-(C1-C4-alkyl)-N-(phenyl-C1-C4-alkyl)aminocarbonyl, N-(C3-C7-cycloalkyl- C1-C4-alkyl)-N-(phenyl-C1-C4-alkyl)aminocarbonyl, N-(C1-C4-alkyl)-N-(C3-C7-cycloalkyl-C1-C4-alkyl)aminocarbonyl, N,N-di-(C1-C4-alkyl)aminocarbonyl, N-(C3-C7-cycloalkyl)-N-(phenyl-C1-C4-alkyl)aminocarbonyl, N-(C3-C7-cycloalkyl)-N-(tetrahydropyranyl-C1-C4-alkyl)aminocarbonyl, N-(C3-C7-cycloalkyl)-N-(tetrahydropyranyl)aminocarbonyl or hydrogen; Rb and Rc are independently selected from a group comprising unsubstituted C1-C4-alkyl, unsubstituted monocyclic aryl, unsubstituted monocyclic heterocyclyl, unsubstituted or substituted monocyclic C3-C7-cycloalkyl, unsubstituted aryl- C1-C4-alkyl, usubstituted monocyclic C3-C7-cycloalkyl- C1-C4-alkyl, hydrogen or acyl, where the acyl is selected from values given in paragraph 1 of the formula of invention; or Rb and Rc together may form a 6-member nitrogen-containing ring which may be unsubstituted or disubstituted with =O; Rd in the fragment of formula (c) denotes a phenyl or phenyl-C1-C4-alkyl; Re denotes hydrogen or C1-C4-alkyl; and m equals 2; each of R4 and R5 denotes hydrogen; and T denotes methylene. The invention also relates to the pharmaceutical composition based on the compound of formula I and a method of treating hypertension using the compound of formula I.

EFFECT: novel pyrrolidine derivatives having renin inhibiting activity are obtained.

7 cl, 19 tbl, 37 ex

 

The text descriptions are given in facsimile form.

1. The compound of formula I:

where R1represents acyl, where the acyl is selected from the following values:
(a) substituted monocyclic arylcarbamoyl, where the aryl fragment selected from phenyl, which is a di - or tizamidine C1-4-alkyl, -O-C1-C4-alkyl, -O-C1-C4-alkylen-O-C1-C4-alkyl, -O-C1-C4-alkylphenyl, -O-C1-C4-alkyl-IT, halo is Yong; -OCF3, -OCF3, -O-C1-C4-alkyl-CF3, -O-C1-C4-alkyl-O-CF3, -O-C1-C4-alkyl-5-membered heterocyclyl containing 1 or 2 heteroatoms N and/or O;
(b) substituted bicyclic heterocalixarenes where heterocyclyl fragment selected from 9-10-membered cyclic system which may be partially saturated or aromatic, and can contain 1 or 2 heteroatoms selected from O and/or N, including indolyl, 2,3-dihydrobenzo[1,4]dioxines where heterocyclyl fragment is mono - or disubstituted With1-C4-alkyl or C1-C4-alkylen-O-C1-C4-alkyl;
R2represents unsubstituted With1-C4-alkyl or C3-C7-cycloalkyl;
R3is a fragment selected from the group of fragments formula:
(a)
;
(b)

(in)

(e)
and
where in any of the fragments of the formulas listed above in (a), (b), (C) and (e), asterisk (*) shows the relationship of the corresponding fragment of R3with the remainder of the molecule in formula I,
Rarepresents N-C1-C4-alkylaminocarbonyl, N-phenylenecarbonyl, N-(phenyl-C1-C4-alkyl)aminocarbonyl, N-(C1-C4-alkyl)-N-(phenyl-C1-C4-alkyl)aminocarbonyl, N-(C3-C7-cycloalkyl-C1-C4-alkyl)-N-(phenyl-C1-C4-alkyl)aminocarbonyl, N-(C1-C4-alkyl)-N-(C3-C7-cycloalkyl-C1-C4-alkyl)aminocarbonyl, N,N-di-(C1-C4-alkyl)aminocarbonyl, N-(C3-C7-cycloalkyl)-N-(phenyl-C1-C4-alkyl)aminocarbonyl, N-(C3-C7-cycloalkyl)-N-(tetrahydropyranyl-C1-C4-alkyl)aminocarbonyl, N-(C3-C7-cycloalkyl)-N-(tetrahydropyranyl)-aminocarbonyl or hydrogen;
Rband Rcindependently selected from the group consisting of unsubstituted With1-C4-alkyl, unsubstituted monocyclic aryl, unsubstituted monocyclic heterocyclyl, unsubstituted or substituted monocyclic3-C7-cycloalkyl, unsubstituted aryl-C1-C4-alkyl, unsubstituted monocyclic3-C7-cycloalkyl-C1-C4-alkyl, hydrogen or acyl, where the acyl is selected from the following values:
(a) mono - or bicyclic arylcarbamoyl, where the aryl fragment selected from phenyl, indanyl, dihydroindole or 1,2,3,4-tetrahydronaphthyl, which is unsubstituted or monosubstituted by heterocyclyl, heterocyclyl-CH2,-O-C1-C4-alkyl, O-C1-C4-alkylen-O-C1-C4the alkyl and/or halogen, where heterotic the ilen fragment in each case represents a monocyclic 5 - or 6-membered heterocyclyl, preferably containing 1 or 2 heteroatoms selected from N and/or O;
(b) mono - or bicyclic heterocalixarenes where heterocyclyl fragment selected from the 5-10-membered cyclic system which may be saturated, partially saturated or aromatic, and can contain 1 or 2 heteroatoms selected from O and/or N, including pyrazinyl, isoxazolyl, pyrrolidinyl, pyrrolidin-2-IMT, tetrahydrofuranyl, tetrahydropyranyl, indolyl, 2,3-dihydrobenzo[1,4]dioxines, bromanil 2N-chromanol, 3,4-dihydro-1H-quinoline-2-IMT, 4,5,6,7-tetrahydrobenzo [d] isoxazolyl, 3A,4,5,6,7,7a-hexahydrobenzo[d]isoxazolyl, 1,4,5,6,-tetrahydrocortisol, 3,4-dihydro-2H-benzo[b][1,4]doxepin, 2H-benzo[b][1,4]oxazin-3-one, dihydroquinoline or 5,6-dihydro-4H-cyclopent[d]isoxazol where heterocyclyl fragment is unsubstituted or monosubstituted by phenyl,1-C4-alkyl or C3-C7-cycloalkyl;
(C) unsubstituted monocyclic cycloalkylcarbonyl where cycloalkenyl fragment selected from C3C4C5With6and C7-cycloalkyl, which may be unsubstituted or monosubstituted O-C1-C4the alkyl or hydroxy;
(g) unsubstituted or substituted alkylaryl, where the alkyl fragment is selected from branched or linear C1-C4-alkyl, where the alkyl fragment is not umestnim or monosubstituted-O-C 1-C4-alkyl, hydroxyl, C1-C4-alkanolamine, aminocarbonyl, N-mono-C1-C4-alkylaminocarbonyl and C1-C4-allyloxycarbonyl;
(d) unsubstituted or substituted mono - or bicyclic aryl-C1-C4-alkylsulphonyl, where the alkyl part may be unsubstituted or monosubstituted by phenyl,1-C4-alkanolamine, O-C1-C4-alkyl or hydroxyl, and where the aryl fragment selected from phenyl or naphthyl which may be unsubstituted or mono-, di - or tizanidine-O-C1-C4-alkyl, halogen-C1-C4the alkyl and/or halogen;
(e) mono - or bicyclic heterocyclyl-C1-C4-alkylsulphonyl where heterocyclyl fragment selected from the 5-10-membered cyclic system which may be saturated, partially saturated or aromatic, and can contain 1 or 2 heteroatoms selected from O and/or N, where heterocyclyl fragment is unsubstituted or monosubstituted =O, -C1-C4-alkyl, amino group or1-C4-alkanoyl, and where the alkyl fragment is unsubstituted or monosubstituted With1-C4-alkyl;
(f) unsubstituted or substituted mono - or bicyclic cycloalkyl-C1-C4-alkylsulphonyl, where the alkyl part may be monosubstituted, including C is the displacement at carbon atom, attached cycloalkenyl fragment With1-C4-alkanolamine, O-C1-C4-alkyl or hydroxyl, and where cycloalkyl fragment selected from C3With5and C6-cycloalkyl, which may be unsubstituted or monosubstituted amino group, O-C1-C4-alkyl or hydroxy;
(C) unsubstituted or substituted allyloxycarbonyl, where the alkyl fragment is selected from branched or linear C1-C4-alkyl which can be monosubstituted by phenyl,-O-C1-C4-alkyl, C1-C4-alkanolamine and N-mono-C1-C4-alkylaminocarbonyl;
(I) unsubstituted mono - or bicyclic aryloxyalkyl, where the aryl fragment selected from phenyl or naphthyl which may be unsubstituted or monosubstituted by heterocyclyl or-O-C1-C4-alkyl, where heterocyclyl fragment represents a monocyclic 5 - or 6-membered heterocyclyl containing 1 or 2 heteroatoms selected from N and/or O, which is unsubstituted or monosubstituted =O;
(C) unsubstituted monocyclic heterocalixarenes where heterocyclyl fragment selected from 5-6-membered cyclic system which may be saturated and may contain 1 heteroatom About, in particular tetrahydropyranyl where heterocyclyl fragment is unsubstituted;
(l) unsubstituted monocyclic cycloalkylcarbonyl where cycloalkenyl fragment selected from C6-cycloalkyl, which is unsubstituted;
(m) unsubstituted or substituted monocyclic aryl-C1-C4-allyloxycarbonyl, where the aryl fragment selected from phenyl, which is unsubstituted or may be disubstituted With1-C4-alkyl;
(h) unsubstituted or substituted monocyclic heterocyclyl-C1-C4-allyloxycarbonyl where heterocyclyl fragment selected from 5-6-membered cyclic system which may be saturated, or aromatic, and can contain 1 or 2 heteroatoms selected from O and/or N, which is unsubstituted or monosubstituted-C1-C4-alkyl or C1-C4-alkanoyl;
(a) unsubstituted or substituted monocyclic cycloalkyl-C1-C4-allyloxycarbonyl, such as cycloalkyl-CH2-where cycloalkenyl fragment selected from C3and C5-cycloalkyl, and may be unsubstituted or substituted, including the substitution at the carbon atom that is attached cycloalkenyl fragment With1-C4-alkyl or C1-C4-alkanolamine;
(p) N-mono - or N,N-di-(unsubstituted mono - or bicyclic aryl, unsubstituted monocyclic3-C7-cycloalkyl, unsubstituted or zames the config monocyclic aryl-C 1-C4-alkyl, unsubstituted monocyclic heterocyclyl-C1-C4-alkyl, unsubstituted monocyclic3-C7-cycloalkyl-C1-C4-alkyl and/or unsubstituted or substituted C1-C4-alkyl)aminocarbonyl, N-mono - or N,N-di-(unsubstituted monocyclic heterocyclyl)aminocarbonyl where heterocyclyl fragment selected from 5-6-membered cyclic system which may be saturated and contains 1 or 2 heteroatoms selected from O and N;
where the alkyl fragment unsubstituted alkylaminocarbonyl represents a branched or linear C1-C4-alkyl, which is unsubstituted;
aryl fragment unsubstituted arylenecarborane represents phenyl or naphthyl, which is unsubstituted;
cycloalkenyl fragment unsubstituted cycloalkylcarbonyl represents a C3and C6-cycloalkyl, which is unsubstituted;
killkenny fragment unsubstituted or substituted arylalkylamines represents aryl-CH2-, aryl-CH2CH2- or aryl-CH(CH2-CH3)-, where the aryl fragment represents phenyl, which is unsubstituted or may be substituted by-O-C1-C4-alkyl or halogen;
heterocyclisation fragment unsubstituted heterocyclyl is killinochchi is heterocyclyl-CH 2where heterocyclyl fragment selected from 5-6-membered cyclic system which may be saturated or aromatic and may contain 1 heteroatom Of which is unsubstituted;
cycloalkylcarbonyl fragment unsubstituted cycloalkylcarbonyl is cycloalkyl-CH2-where cycloalkenyl fragment selected from C6-cycloalkyl, which is unsubstituted;
or Rband Rcmay together form a 6-membered nitrogen cycle, which may be unsubstituted or disubstituted =O;
Rdin the fragment of the formula (I) represents a phenyl or phenyl-C1-C4-alkyl;
Rerepresents hydrogen or C1-C4-alkyl; and
m is 2;
each of R4and R5represents hydrogen; and
and T represents a methylene;
or its pharmaceutically acceptable salt.

2. The compound of formula I according to claim 1, where
R1represents acyl;
R2represents; unsubstituted With1-C4-alkyl or C3-C7-cycloalkyl;
R3is a fragment selected from the group of fragments formula:
(a);
(b)

(in)

and (e)

where in any of the fragments of the formulas above is (a), (b), (C) and (e), asterisk (*) shows the relationship of the corresponding fragment of R3with the remainder of the molecule in formula I,
Rarepresents N-C1-C4-alkylaminocarbonyl, N-phenylenecarbonyl, N-(phenyl-C1-C4-alkyl)aminocarbonyl, N-(C1-C4-alkyl)-N-(phenyl-C1-C4-alkyl)aminocarbonyl, N-(C3-C7-cycloalkyl-C1-C4-alkyl)-N-(phenyl-C1-C4-alkyl)aminocarbonyl, N-(C1-C4-alkyl)-N-(C3-C7-cycloalkyl-C1-C4-alkyl)aminocarbonyl, N,N-di-(C1-C4-alkyl)aminocarbonyl, N-(C3-C7-cycloalkyl)-N-(phenyl-C1-C4-alkyl)aminocarbonyl, N-(C3-C7-cycloalkyl)-N-(tetrahydropyranyl-C1-C4-alkyl)aminocarbonyl, N-(C3-C7-cycloalkyl)-N-(tetrahydropyranyl)aminocarbonyl or hydrogen;
Rbrepresents unsubstituted With1-C4-alkyl, unsubstituted monocyclic aryl, unsubstituted aryl-C1-C4-alkyl or acyl;
Rcrepresents a C3-C7-cycloalkyl, hydrogen or C1-C4-alkyl;
Rdrepresents phenyl-C1-C4-alkyl;
Rerepresents hydrogen or C1-C4-alkyl; and
m is 2;
each of R4and R5represents hydrogen; and
and T is the Wallpaper methylene;
or its pharmaceutically acceptable salt.

3. The compound of formula I according to claim 1, where
R1represents acyl;
R2represents a C3-C7-cycloalkyl or1-C4-alkyl;
R3is a fragment selected from the group of fragments formula:
(a)
;
(b)

(in)
and
(e)

where in any of the fragments of formulae given above in (a), (b), (C) and (e), asterisk (*) shows the relationship of the corresponding fragment of R3with the remainder of the molecule in formula I,
Rarepresents hydrogen or N-C1-C4-alkylaminocarbonyl, N-phenylenecarbonyl, N-(phenyl-C1-C4-alkyl)aminocarbonyl, N-(C1-C4-alkyl)-N-(phenyl-C1-C4-alkyl)aminocarbonyl, N-(C3-C7-cycloalkyl-C1-C4-alkyl)-N-(phenyl-C1-C4-alkyl)aminocarbonyl, N-(C1-C4-alkyl)-N-(C3-C7-cycloalkyl-C1-C4-alkyl)aminocarbonyl, N,N-di(C1-C4-alkyl)aminocarbonyl, N-(C3-C7-cycloalkyl)-N-(phenyl-C1-C4-alkyl)aminocarbonyl, N-(C3-C7-cycloalkyl)-N-(tetrahydropyranyl-C1-C4-alkyl)aminocarbonyl, N-(C3-C7-cycloalkyl)-N-(tetrahydropyranyl)aminocarb the sludge;
each of Rband Rcindependently from each other selected from hydrogen, C1-C4-alkyl, C3-C7-cycloalkyl-C1-C4-alkyl, C3-C7-cycloalkyl, unsubstituted aryl, naphthyl, naphthyl-C1-C4the alkyl or acyl where the acyl is selected from the following values:
(a) mono - or bicyclic arylcarbamoyl, where the aryl fragment selected from phenyl, indanyl, dihydroindole or 1,2,3,4-tetrahydronaphthyl, which is unsubstituted, monosubstituted by heterocyclyl, heterocyclyl-CH2, -O-C1-C4-alkyl, O-C1-C4-alkylen-O-C1-C4the alkyl and/or halogen, where heterocyclyl fragment in each case represents a monocyclic 5 - or 6-membered heterocyclyl, preferably containing 1 or 2 heteroatoms selected from N and/or O;
(b) mono - or bicyclic heterocalixarenes where heterocyclyl fragment selected from the 5-10-membered cyclic system which may be saturated, partially saturated or aromatic, and can contain 1 or 2 heteroatoms selected from O and/or N, including pyrazinyl, isoxazolyl, pyrrolidinyl, pyrrolidin-2-IMT, tetrahydrofuranyl, tetrahydropyranyl, indolyl, 2,3-dihydrobenzo[1,4]dioxines, bromanil 2N-chromanol, 3,4-dihydro-1H-quinoline-2-IMT, 4,5,6,7-tetrahydrobenzo[d]isoxazolyl, 3A,4,5,6,7,7a-hexahydro is Enzo[d]isoxazolyl, 1,4,5,6,-tetrahydrocortisol, 3,4-dihydro-2H-benzo[b][1,4]doxepin, 2H-benzo[b]-[1,4]oxazin-3-one, dihydroquinoline or 5,6-dihydro-4H-cyclopent[d]isoxazol where heterocyclyl fragment is unsubstituted or monosubstituted by phenyl,1-C4-alkyl or C3-C7-cycloalkyl;
(C) unsubstituted monocyclic cycloalkylcarbonyl where cycloalkenyl fragment selected from C3C4With5With6and C7-cycloalkyl, which may be unsubstituted or monosubstituted O-C1-C4-alkyl or hydroxy;
(g) unsubstituted or substituted alkylaryl, where the alkyl fragment is selected from branched or linear C1-C4-alkyl, where the alkyl fragment is unsubstituted or monosubstituted-O-C1-C4-alkyl, hydroxyl, C1-C4-alkanolamine, aminocarbonyl, N-mono-C1-C4-alkylaminocarbonyl and C1-C4-allyloxycarbonyl;
(d) unsubstituted or substituted mono - or bicyclic aryl-C1-C4-alkylsulphonyl, where the alkyl part may be unsubstituted or monosubstituted by phenyl,1-C4-alkanolamine, O-C1-C4-alkyl or hydroxyl, and where the aryl fragment selected from phenyl or naphthyl which may be unsubstituted or mono-, di - or tizanidine-O-is 1-C4-alkyl, halogen-C1-C4the alkyl and/or halogen;
(e) mono - or bicyclic heterocyclyl-C1-C4-alkylsulphonyl where heterocyclyl fragment selected from the 5-10-membered cyclic system which may be saturated, partially saturated or aromatic, and can contain 1 or 2 heteroatoms selected from O and/or N, where heterocyclyl fragment is unsubstituted or monosubstituted =O, -C1-C4-alkyl, amino group or C1-C4-alkanoyl, and where the alkyl fragment is unsubstituted or monosubstituted With1-C4-alkyl;
(f) unsubstituted or substituted mono - or bicyclic cycloalkyl-C1-C4-alkylsulphonyl, where the alkyl part may be monosubstituted, including substitution at the carbon atom that is attached cycloalkenyl fragment With1-C4-alkanolamine, O-C1-C4-alkyl or hydroxyl, and where cycloalkyl fragment selected from C3With5and C6-cycloalkyl, which may be unsubstituted or monosubstituted amino group, O-C1-C4-alkyl or hydroxy;
(C) unsubstituted or substituted allyloxycarbonyl, where the alkyl fragment is selected from branched or linear C1-C4-alkyl which can be monosubstituted by phenyl, -O-C1-C4-what Kilom, With1-C4-alkanolamine and N-mono-C1-C4-alkylaminocarbonyl;
(I) unsubstituted mono - or bicyclic aryloxyalkyl, where the aryl fragment selected from phenyl or naphthyl which may be unsubstituted or monosubstituted by heterocyclyl or-O-C1-C4-alkyl, where heterocyclyl fragment represents a monocyclic 5 - or 6-membered heterocyclyl containing 1 or 2 heteroatoms selected from N and/or O, which is unsubstituted or monosubstituted =O;
(C) unsubstituted monocyclic heterocalixarenes where heterocyclyl fragment selected from 5-6-membered cyclic system which may be saturated and may contain 1 heteroatom About, in particular tetrahydropyranyl where heterocyclyl fragment is unsubstituted;
(l) unsubstituted monocyclic cycloalkylcarbonyl where cycloalkenyl fragment selected from C6-cycloalkyl, which is unsubstituted;
(m) unsubstituted or substituted monocyclic aryl-C1-C4-allyloxycarbonyl, where the aryl fragment selected from phenyl, which is unsubstituted or may be disubstituted With1-C4-alkyl;
(h) unsubstituted or substituted monocyclic heterocyclyl-C1-C4-allyloxycarbonyl where heterocyclyl fragment selected from 5-6-membered CEC is practical system, which may be saturated, or aromatic, and can contain 1 or 2 heteroatoms selected from O and/or N, which is unsubstituted or monosubstituted-C1-C4-alkyl or C1-C4-alkanoyl;
(a) unsubstituted or substituted monocyclic cycloalkyl-C1-C4-allyloxycarbonyl, such as cycloalkyl-CH2-where cycloalkenyl fragment selected from C3and C5-cycloalkyl, which may be unsubstituted or substituted, including the substitution at the carbon atom that is attached cycloalkenyl fragment With1-C4-alkyl or C1-C4-alkanolamine;
(p) N-mono - or N,N-di-(unsubstituted mono - or bicyclic aryl, unsubstituted monocyclic3-C7-cycloalkyl, unsubstituted or substituted monocyclic aryl-C1-C4-alkyl, unsubstituted monocyclic heterocyclyl-C1-C4-alkyl, unsubstituted monocyclic3-C7-cycloalkyl-C1-C4-alkyl and/or unsubstituted or substituted C1-C4-alkyl)aminocarbonyl, N-mono - or N,N-di-(unsubstituted monocyclic heterocyclyl)aminocarbonyl where heterocyclyl fragment selected from 5-6-membered cyclic system which may be saturated and contains 1 or 2 heteroatoms selected from O and N;
where the alkyl fragment resumes the frame of alkylaminocarbonyl represents a branched or linear C 1-C4-alkyl, which is unsubstituted;
aryl fragment unsubstituted arylenecarborane represents phenyl or naphthyl, which is unsubstituted;
cycloalkenyl fragment unsubstituted cycloalkylcarbonyl represents a C3and C6-cycloalkyl, which is unsubstituted;
killkenny fragment unsubstituted or substituted arylalkylamines represents aryl-CH2-, aryl-CH2CH2- or aryl-CH(CH2-CH3)-, where the aryl fragment represents phenyl, which is unsubstituted or may be substituted by-O-C1-C4-alkyl or halogen;
heterocyclisation fragment unsubstituted geterotsiklicheskikh is heterocyclyl-CH2where heterocyclyl fragment selected from 5-6-membered cyclic system which may be saturated or aromatic and may contain 1 heteroatom Of which is unsubstituted;
cycloalkylcarbonyl fragment unsubstituted cycloalkylcarbonyl is cycloalkyl-CH2-where cycloalkenyl fragment selected from C6-cycloalkyl, which is unsubstituted;
Rdrepresents phenyl or phenyl-C1-C4-alkyl;
Rerepresents hydrogen; and
m denotes 2
each of R4and R5represents hydrogen; and
and T represents a methylene;
or its pharmaceutically acceptable salt.

4. The compound of formula I according to claim 1, selected from the group including
N-((3S*,4S*)-4-{[(3-acetylamino-3-methylbutyryl)cyclopropylamino]methyl}pyrrolidin-3-ylmethyl)-N-isopropyl-4-methoxy-3-(3-methoxypropane)benzamid,
N-[(3S*,4S*)-4-({cyclopropyl-[2-(2-oxo-pyrrolidin-1-yl)acetyl]amino}methyl)pyrrolidin-3-ylmethyl]-N-isopropyl-4-methoxy-3-(3-methoxypropane)benzamid,
N-[(3S*,4S*)-4-({[2-(1-acetylaminophenol)acetyl]cyclopropylamino}methyl)pyrrolidin-3-ylmethyl]-N-isopropyl-4-methoxy-3-(3-methoxypropane)benzamid,
N-((3S*,4S*)-4-{[cyclopropyl-(3,3-dimethylbutyryl)amino]methyl}pyrrolidin-3-ylmethyl)-N-isopropyl-4-methoxy-3-(3-methoxypropane)benzamid,
N-[(3S*,4S*)-4-({[2-(1-acetylaminophenol)acetyl]cyclopropylamino}methyl)pyrrolidin-3-ylmethyl]-N-isopropyl-4-methoxy-3-(3-methoxypropane)benzamid,
N-((3S*,4S*)-4-{[cyclopropyl-(3-methyl-3-pyrrol-1-albuterol)amino]methyl}pyrrolidin-3-ylmethyl)-N-isopropyl-4-methoxy-3-(3-methoxypropane)benzamid,
N-[(3S*,4S*)-4-({cyclopropyl-[2-(3-oxo-3,4-dihydro-2H-benzo[1,4]oxazin-6-yl)acetyl]amino}methyl)pyrrolidin-3-ylmethyl]-N-isopropyl-4-methoxy-3-(3-methoxypropane)benzamid,
N-[(3S*,4S*)-4-({cyclopropyl-[2-(1-isobutyleneisoprene)acetyl]amino}methyl)pyrrolidin-3-ylmethyl]-N-isopropyl-4-methoxy-3-(3-methoxypropane)b is same,
N-((3S*,4S*)-4-{[cyclopropyl-(4-
methylpentanol)amino]methyl }pyrrolidin-3-ylmethyl)-N-isopropyl-4-methoxy-3-(3-methoxypropane)benzamid,
N-[(3S*,4S*)-4-({cyclopropyl-[2-(2-methylbenzothiazol-5-yl)acetyl]amino}methyl)pyrrolidin-3-ylmethyl]-N-isopropyl-4-methoxy-3-(3-methoxypropane)benzamid,
N-((3S*,4S*)-4-{[(3-cyclohexylpropionic)cyclopropylamino]methyl}pyrrolidin-3-ylmethyl)-N-isopropyl-4-methoxy-3-(3-methoxypropane)benzamid,
N-((3S,4S)-4-{[cyclopropyl-(3-cyclopropylmethyl)amino]methyl}pyrrolidin-3-ylmethyl)-N-isopropyl-4-methoxy-3-(3-methoxypropane)benzamid,
N-((3S,4S)-4-{[(3-cyclopentylpropionyl)cyclopropylamino]methyl}-pyrrolidin-3-ylmethyl)-N-isopropyl-4-methoxy-3-(3-methoxypropane)benzamid,
N-((3S,4S)-4-{[cyclopropyl-(3,3-diphenylpropyl)amino]methyl}pyrrolidin-3-ylmethyl)-N-isopropyl-4-methoxy-3-(3-methoxypropane)benzamid,
N-[(3S,4S)-4-({cyclopropyl-[2-(2,6-dimethylphenoxy)acetyl]amino}methyl)pyrrolidin-3-ylmethyl]-N-isopropyl-4-methoxy-3-(3-methoxypropane)benzamid,
N-((3S,4S)-4-{[cyclopropyl-((S)-3-phenylbutyl)amino]methyl}pyrrolidin-3-ylmethyl)-N-isopropyl-4-methoxy-3-(3-methoxypropane)benzamid,
N-[(3S,4S)-4-({[2-(1-acetylpiperidine-4-yl)acetyl]cyclopropylamino}methyl)pyrrolidin-3-ylmethyl]-N-isopropyl-4-methoxy-3-(3-methoxypropane)benzamid,
N-((3S,4S)-4-{[((S)-3-acetylamino-3-phenylpropionyl)cyclopropylamino]methyl}pyrrolidin-3-ylmethyl)-N-isopropyl-4-methoxy-3-(3-methoxypropane)benzo the Ministry of foreign Affairs,
N-((3S,4S)-4-{[((R)-3-acetylamino-3-phenylpropionyl)cyclopropylamino]methyl}pyrrolidin-3-ylmethyl)-N-isopropyl-4-methoxy-3-(3-methoxypropane)benzamid,
N-((3S,4S)-4-{[cyclopropyl-((R)-3-hydroxy-3-phenylpropionyl)amino]methyl}pyrrolidin-3-ylmethyl)-N-isopropyl-4-methoxy-3-(3-methoxypropane)benzamid,
N-((3S,4S)-4-{[cyclopropyl-((S)-3-hydroxy-3-phenylpropionyl)amino]methyl}pyrrolidin-3-ylmethyl)-N-isopropyl-4-methoxy-3-(3-methoxypropane)benzamid,
N - ((3S,4S)-4-{[cyclopropyl-(3-furan-2-ylpropyl)amino]methyl}pyrrolidin-3-ylmethyl)-N-isopropyl-4-methoxy-3-(3-methoxypropane)benzamid,
N-((3S,4S)-4-{[cyclopropyl-(2-furan-2-ylacetic)amino]methyl}pyrrolidin-3-ylmethyl)-N-isopropyl-4-methoxy-3-(3-methoxypropane)benzamid,
N-((3S,4S)-4-{[cyclopropyl-((S)-2-methoxy-2-cyclohexylethyl)amino]methyl}pyrrolidin-3-ylmethyl)-N-isopropyl-4-methoxy-3-(3-methoxypropane)benzamid,
N-((3S,4S)-4-{[cyclopropyl-((S)-2-hydroxy-4-methylpentanoic)amino]methyl}pyrrolidin-3-ylmethyl)-N-isopropyl-4-methoxy-3-(3-methoxypropane)benzamid,
N-{(3S*,4S*)-4-[(cyclohexanecarbonitrile)methyl]pyrrolidin-3-ylmethyl}-N-isopropyl-4-methoxy-3-(3-methoxypropane)benzamide
cyclopropyl-[(3S,4S)-4-({isopropyl-[4-methoxy-3-(3-methoxypropane)benzoyl]amino}methyl)pyrrolidin-3-ylmethyl]amide cycloheptanone acid,
N-((3S,4S)-4-{[(2-cyclopentylacetyl)cyclopropylamino]methyl}pyrrolidin-3-ylmethyl)-N-isopropyl-4-methoxy-3-(3-methoxypropyl the XI)benzamid,
N-((3S*,4S*)-4-{[(2-cyclohexylethyl)cyclopropylamino]methyl}pyrrolidin-3-ylmethyl)-N-isopropyl-4-methoxy-3-(3-methoxypropane)benzamid,
N-{(3S*,4S*)-4-[(benzoylthiophene)methyl]pyrrolidin-3-ylmethyl}-N-isopropyl-4-methoxy-3-(3-methoxypropane)benzamid,
N-[(3S*,4S*)-4-({cyclopropyl-[2-(4-fluoro-phenyl)acetyl]amino}methyl)pyrrolidin-3-ylmethyl]-N-isopropyl-4-methoxy-3-(3-methoxypropane)benzamid,
N-[(3S,4S)-4-({[2-(4-chlorophenyl)acetyl]cyclopropylamino}methyl)pyrrolidin-3-ylmethyl]-N-isopropyl-4-methoxy-3-(3-methoxypropane)benzamid,
N-[(3S*,4S*)-4-({[2-(3-chlorophenyl)acetyl]cyclopropylamino}methyl)pyrrolidin-3-ylmethyl]-N-isopropyl-4-methoxy-3-(3-methoxypropane)benzamid,
N-[(3S*,4S*)-4-({cyclopropyl-[2-(2-methoxyphenyl)acetyl]amino}methyl)pyrrolidin-3-ylmethyl]-N-isopropyl-4-methoxy-3-(3-methoxypropane)benzamid,
N-[(3S*,4S*)-4-({cyclopropyl-[2-(3,5-debtor-phenyl)acetyl]amino}methyl)pyrrolidin-3-ylmethyl]-N-isopropyl-4-methoxy-3-(3-methoxypropane)benzamid,
N-[(3S*,4S*)-4-({cyclopropyl-[2-(2,3,5-Cryptor-phenyl)acetyl]amino}methyl)pyrrolidin-3-ylmethyl]-N-isopropyl-4-methoxy-3-(3-methoxypropane)benzamid,
N-[(3S*,4S*)-4-({cyclopropyl-[2-(3-triptoreline)acetyl]amino}methyl)pyrrolidin-3-ylmethyl]-N-isopropyl-4-methoxy-3-(3-methoxypropane)benzamid,
N-[(3S*,4S*)-4-({[2-(3,5-bis-triptoreline)acetyl]cyclopropylamino}methyl)pyrrolidin-3-ylmethyl]-N-isopropyl-4-methoxy-3-(3-methoxypropane)benzamid,
N-((3S*,4S*)-4-{[qi is sapropel-(3-pyrrolidin-1-aventyl)amino]methyl}pyrrolidin-3-ylmethyl)-N-isopropyl-4-methoxy-3-(3-methoxypropane)benzamid,
N-[(3S*,4S*)-4-({cyclopropyl-[2-(3'-fluoro-biphenyl-3-yl)acetyl]amino}methyl)pyrrolidin-3-ylmethyl]-N-isopropyl-4-methoxy-3-(3-methoxypropane)benzamid,
N-((3S*,4S*)-4-{[cyclopropyl-(3-chloro-6-methoxy-1-aventyl)amino]methyl}pyrrolidin-3-ylmethyl)-N-isopropyl-4-methoxy-3-(3-methoxypropane)benzamid,
N-((3S*,4S*)-4-{[cyclopropyl-(4-(morpholine-4-iletilmistir)amino]methyl}pyrrolidin-3-ylmethyl)-N-isopropyl-4-methoxy-3-(3-methoxypropane)benzamid,
cyclopropyl-[(3S*,4S*)-4-({isopropyl-[4-methoxy-3-(3-methoxypropane)benzoyl]amino}methyl)pyrrolidin-3-ylmethyl]amide of 1H-indole-2-carboxylic acid,
cyclopropyl-[(3S*,4S*)-4-({isopropyl-[4-methoxy-3-(3-methoxypropane)benzoyl]amino}methyl)pyrrolidin-3-ylmethyl]amide of 1H-indole-3-carboxylic acid,
cyclopropyl-[(3S,4S)-4-({isopropyl-[4-methoxy-3-(3-methoxypropane)benzoyl]amino}methyl)pyrrolidin-3-ylmethyl]amide 2,3-dihydrobenzo[1,4]dioxin-6-carboxylic acid,
N-((3S*,4S*)-4-{[cyclopropyl-(2-naphthalene-2-ylacetic)amino]methyl}pyrrolidin-3-ylmethyl)-N-isopropyl-4-methoxy-3-(3-methoxypropane)benzamid,
N-((3S,4S)-4-{[cyclopropyl-(2-phenoxyacetyl)amino]methyl}pyrrolidin-3-ylmethyl)-N-isopropyl-4-methoxy-3-(3-methoxypropane)benzamid,
N-((3S*,4S*)-4-{[cyclopropyl-((S)-2-phenylpropionyl)amino]methyl}pyrrolidin-3-ylmethyl)-N-isopropyl-4-methoxy-3-(3-methoxypropane)benzamid,
N-((3S*,4S*)-4-{[cyclopropyl-((R)-2-phenylpropionyl)amino]methyl}pyrrolidin-3-ylmethyl)-N-isopropyl-4-methoxy-3-(3-m is oxypropane)benzamid,
N-((3S,4S)-4-{[cyclopropyl-((S)-2-hydroxy-2-phenylacetyl)amino]methyl}pyrrolidin-3-ylmethyl)-N-isopropyl-4-methoxy-3-(3-methoxypropane)benzamid,
N-((3S,4S)-4-{[cyclopropyl-((R)-2-hydroxy-2-phenylacetyl)amino]methyl}pyrrolidin-3-ylmethyl)-N-isopropyl-4-methoxy-3-(3-methoxypropane)benzamid,
N-((3S,4S)-4-{[cyclopropyl-((R)-2-methoxy-2-phenylacetyl)amino]methyl}pyrrolidin-3-ylmethyl)-N-isopropyl-4-methoxy-3-(3-methoxypropane)benzamid,
N-((3S,4S)-4-{[cyclopropyl-((S)-2-methoxy-2-phenylacetyl)amino]methyl}pyrrolidin-3-ylmethyl)-N-isopropyl-4-methoxy-3-(3-methoxypropane)benzamid,
cyclopropyl-[(3S*,4S*)-4-({isopropyl-[4-methoxy-3-(3-methoxypropane)benzoyl]amino}methyl)pyrrolidin-3-ylmethyl]amide tetrahydrofuran-3-carboxylic acid,
cyclopropyl-[(3S*,4S*)-4-({isopropyl-[4-methoxy-3-(3-methoxypropane)benzoyl]amino}methyl)pyrrolidin-3-ylmethyl]amide tetrahydrofuran-2-carboxylic acid,
cyclopropyl-[(3S,4S)-4-({isopropyl-[4-methoxy-3-(3-methoxypropane)benzoyl]amino}methyl)pyrrolidin-3-ylmethyl]amide (S)-tetrahydropyran-3-carboxylic acid,
cyclopropyl-[(3S,4S)-4-({isopropyl-[4-methoxy-3-(3-methoxypropane)benzoyl]amino}methyl)pyrrolidin-3-ylmethyl]amide (R)-tetrahydropyran-3-carboxylic acid,
cyclopropyl-[(3S*,4S*)-4-({isopropyl-[4-methoxy-3-(3-methoxypropane)benzoyl]amino}methyl)pyrrolidin-3-ylmethyl]amide tetrahydropyran-4-carboxylic acid,
N-((3S,4S)-4-{[cyclopropyl-(4-hydroxycyclohexane the Nile)amino]methyl}pyrrolidin-3-ylmethyl)-N-isopropyl-4-methoxy-3-(3-methoxypropane)benzamid,
N-((3S,4S)-4-{[cyclopropyl-(CIS-4-methoxycyclohexanone)amino]methyl}pyrrolidin-3-ylmethyl)-N-isopropyl-4-methoxy-3-(3-methoxypropane)benzamid,
N-((3S,4S)-4-{[cyclopropyl-(TRANS-4-methoxycyclohexanone)amino]methyl}pyrrolidin-3-ylmethyl)-N-isopropyl-4-methoxy-3-(3-methoxypropane)benzamid,
N-((3S,4S)-4-{[cyclopropyl-((S)-2-tetrahydrofuran-2-ylacetic)amino]methyl}pyrrolidin-3-ylmethyl)-N-isopropyl-4-methoxy-3-(3-methoxypropane)benzamid,
N-((3S,4S)-4-{[cyclopropyl-((R)-2-tetrahydrofuran-2-ylacetic)amino]methyl}pyrrolidin-3-ylmethyl)-N-isopropyl-4-methoxy-3-(3-methoxypropane)benzamid,
N-((3S,4S)-4-{[cyclopropyl-((S)-2-tetrahydropyran-2-ylacetic)amino]methyl}pyrrolidin-3-ylmethyl)-N-isopropyl-4-methoxy-3-(3-methoxypropane)benzamid,
N-((3S,4S)-4-{[cyclopropyl-((R)-2-tetrahydropyran-2-ylacetic)amino]methyl}pyrrolidin-3-ylmethyl)-N-isopropyl-4-methoxy-3-(3-methoxypropane)benzamid,
cyclopropyl-[(3S,4S)-4-({isopropyl-[4-methoxy-3-(3-methoxypropane)benzoyl]amino}methyl)pyrrolidin-3-ylmethyl]amide (R)-1,2,3,4-tetrahydronaphthalen-2-carboxylic acid,
cyclopropyl-[(3S,4S)-4-({isopropyl-[4-methoxy-3-(3-methoxypropane)benzoyl]amino}methyl)pyrrolidin-3-ylmethyl]amide (S)-1,2,3,4-tetrahydronaphthalen-2-carboxylic acid,
N-((3S*,4S*)-4-{[cyclopropyl-(2-tetrahydropyran-4-ylacetic)amino]methyl}pyrrolidin-3-ylmethyl)-N-isopropyl-4-methoxy-3-(3-methoxypropane)benzamid,
cyclopropyl-[(3S,4S)-4-({isopropyl-[4-m is toxi-3-(3-methoxypropane)benzoyl]amino}methyl)pyrrolidin-3-ylmethyl]amide chroman-2-carboxylic acid,
cyclopropyl-[(3S,4S)-4-({isopropyl-[4-methoxy-3-(3-methoxypropane)benzoyl]amino}methyl)pyrrolidin-3-ylmethyl]amide 2H-chromen-3-carboxylic acid,
cyclopropyl-[(3S,4S)-4-({isopropyl-[4-methoxy-3-(3-methoxypropane)benzoyl]amino}methyl)pyrrolidin-3-ylmethyl]amide (R)-2,3-dihydrobenzo[1,4]dioxin-2-carboxylic acid,
cyclopropyl-[(3S,4S)-4-({isopropyl-[4-methoxy-3-(3-methoxypropane)benzoyl]amino}methyl)pyrrolidin-3-ylmethyl]amide (S)-2,3-dihydrobenzo[1,4]dioxin-2-carboxylic acid,
cyclopropyl-[(3S,4S)-4-({isopropyl-[4-methoxy-3-(3-methoxypropane)benzoyl]amino}methyl)pyrrolidin-3-ylmethyl]amide 2-oxo-1,2,3,4-tetrahydroquinolin-4-carboxylic acid,
cyclopropyl-[(3S,4S)-4-({isopropyl-[4-methoxy-3-(3-methoxypropane)benzoyl]amino}methyl)pyrrolidin-3-ylmethyl]amide 4,5,6,7-tetrahydrobenzo[d]isoxazol-3-carboxylic acid,
cyclopropyl-[(3S,4S)-4-({isopropyl-[4-methoxy-3-(3-methoxypropane)benzoyl]amino}methyl)pyrrolidin-3-ylmethyl]amide 3A,4,5,6,7,7a-hexahydrobenzo[d]isoxazol-3-carboxylic acid,
N-((3S,4S)-4-{[(2-benzo[d]isoxazol-3-ylacetic)cyclopropylamino]methyl}pyrrolidin-3-ylmethyl)-N-isopropyl-4-methoxy-3-(3-methoxypropane)benzamid,
cyclopropyl-[(3S*,4S*)-4-({isopropyl-[4-methoxy-3-(3-methoxypropane)benzoyl]amino}methyl)pyrrolidin-3-ylmethyl]amide 1,4,5,6-tetrahydrocyclopent-3-carboxylic acid,
cyclopropyl-[(3S*,4S*)-4-({isopropyl-[4-methoxy-3-(3-methoxypropane)benzoyl]amino}is ethyl)pyrrolidin-3-ylmethyl]amide isoxazol-3-carboxylic acid,
cyclopropyl-[(3S*,4S*)-4-({isopropyl-[4-methoxy-3-(3-methoxypropane)benzoyl]amino}methyl)pyrrolidin-3-ylmethyl]amide 5-methylisoxazol-3-carboxylic acid,
cyclopropyl-[(3S*,4S*)-4-({isopropyl-[4-methoxy-3-(3-methoxypropane)benzoyl]amino}methyl)pyrrolidin-3-ylmethyl]amide 5-cyclopropylmethoxy-3-carboxylic acid,
cyclopropyl-[(3S,4S)-4-({isopropyl-[4-methoxy-3-(3-methoxypropane)benzoyl]amino}methyl)pyrrolidin-3-ylmethyl]amide 5-phenylisoxazol-3-carboxylic acid,
cyclopropyl-[(3S*,4S*)-4-({isopropyl-[4-methoxy-3-(3-methoxypropane)benzoyl]amino}methyl)pyrrolidin-3-ylmethyl]amide 5-methylpyrazine-2-carboxylic acid,
cyclopropyl-[(3S,4S)-4-({isopropyl-[4-methoxy-3-(3-methoxypropane)benzoyl]amino}methyl)pyrrolidin-3-ylmethyl]amide indan-2-carboxylic acid,
cyclopropyl-[(3S*,4S*)-4-({isopropyl-[4-methoxy-3-(3-methoxypropane)benzoyl]amino}methyl)pyrrolidin-3-ylmethyl]amide 5-oxo-1-phenylpyrrolidine-3-carboxylic acid,
N-cyclopropyl-N-[(3S*,4S*)-4-({isopropyl-[4-methoxy-3-(3-methoxypropane)benzoyl]amino}methyl)pyrrolidin-3-ylmethyl]succinamic,
N-cyclopropyl-N-[(3S*,4S*)-4-({isopropyl-[4-methoxy-3-(3-methoxypropane)benzoyl]amino}methyl)pyrrolidin-3-ylmethyl]-N'-methylsuccinimide,
methyl ester of N-cyclopropyl-N-[(3S*,4S*)-4-({isopropyl-[4-methoxy-3-(3-methoxypropane)benzoyl]amino}methyl)pyrrolidin-3-ylmethyl]succinamide acid,
N-((3S,4S)-4-{[cyclopropyl-(2-piperidine-4-ylacetic)AMI is about]methyl}pyrrolidin-3-ylmethyl)-N-isopropyl-4-methoxy-3-(3-methoxypropane)benzamid,
N-[(3S,4S)-4-({[2-(4-aminocyclohexane)acetyl]cyclopropylamino}methyl)pyrrolidin-3-ylmethyl]-N-isopropyl-4-methoxy-3-(3-methoxypropane)benzamid,
N-[(3S,4S)-4-({[2-(4-aminocyclohexane)acetyl]cyclopropylamino}methyl)pyrrolidin-3-ylmethyl]-N-isopropyl-4-methoxy-3-(3-methoxypropane)benzamid,
N-((3S,4S)-4-{[cyclopropyl-(2-methyl-2-phenylpropionyl)amino]methyl}pyrrolidin-3-ylmethyl)-N-isopropyl-4-methoxy-3-(3-methoxypropane)benzamid,
N-((3S,4S)-4-{[((S)-2-hydroxy-2-phenylacetyl)methylamino]methyl}pyrrolidin-3-ylmethyl)-N-isopropyl-4-methoxy-3-(3-methoxypropane)benzamid,
N-((3S,4S)-4-{[((S)-2-methoxy-2-phenylacetyl)methylamino]methyl}pyrrolidin-3-ylmethyl)-N-isopropyl-4-methoxy-3-(3-methoxypropane)benzamid,
N-((3S,4S)-4-{[((S)-2-hydroxy-4-methylpentanoic)methylamino]methyl}pyrrolidin-3-ylmethyl)-N-isopropyl-4-methoxy-3-(3-methoxypropane)benzamid,
N-((3S,4S)-4-{[((S)-2-methoxy-2-cyclohexylethyl)methylamino]methyl}pyrrolidin-3-ylmethyl)-N-isopropyl-4-methoxy-3-(3-methoxypropane)benzamid,
N-((3S,4S)-4-{[((S)-2-hydroxy-3-methylbutyryl)methylamino]methyl}pyrrolidin-3-ylmethyl)-N-isopropyl-4-methoxy-3-(3-methoxypropane)benzamid,
N-((3S,4S)-4-{[((S)-2-hydroxy-3-phenylpropionyl)methylamino]methyl}pyrrolidin-3-ylmethyl)-N-isopropyl-4-methoxy-3-(3-methoxypropane)benzamid,
N-((3S,4S)-4-{[((S)-2-cyclohexyl-2-hydroxyacetic)methylamino]methyl}pyrrolidin-3-ylmethyl)-N-isopropyl-4-methoxy-3-(3-methoxypropane)benzamid,
N-((3S,4S)-4-{[((S)-3-Ki-the Roxy-3-phenylpropionyl)methylamino]methyl}pyrrolidin-3-ylmethyl)-N-isopropyl-4-methoxy-3-(3-methoxypropane)benzamid,
N-((3S,4S)-4-{[((R)-3-hydroxy-3-phenylpropionyl)methylamino]methyl}pyrrolidin-3-ylmethyl)-N-isopropyl-4-methoxy-3-(3-methoxypropane)benzamid,
N-((3S,4S)-4-{[(2-furan-2-ylacetic)methylamino]methyl}pyrrolidin-3-ylmethyl)-N-isopropyl-4-methoxy-3-(3-methoxypropane)benzamid,
N-((3S,4S)-4-{[((S)-2-methoxy-3-methylbutyryl)methylamino]methyl}pyrrolidin-3-ylmethyl)-N-isopropyl-4-methoxy-3-(3-methoxypropane)benzamid,
N-((3S,4S)-4-{[((S)-2-methoxy-4-methylpentanol)methylamino]methyl}pyrrolidin-3-ylmethyl)-N-isopropyl-4-methoxy-3-(3-methoxypropane)benzamid,
N-{(3S*,4S*)-4-[(benzoylamino)methyl]pyrrolidin-3-ylmethyl}-N-isopropyl-4-methoxy-3-(3-methoxypropane)benzamid,
N-((3S,4S)-4-{[(2-cyclohexylethyl)methylamino]methyl}pyrrolidin-3-ylmethyl)-N-isopropyl-4-methoxy-3-(3-methoxypropane)benzamid,
N-isopropyl-4-methoxy-N-[(3S*,4S*)-4-({[2-(3-methoxyphenyl)acetyl]methylamino}methyl)pyrrolidin-3-ylmethyl]-3-(3-methoxypropane)benzamid,
[(3S,4S)-4-({isopropyl-[4-methoxy-3-(3-methoxypropane)benzoyl]amino}methyl)pyrrolidin-3-ylmethyl]methylamide indan-2-carboxylic acid,
[(3S,4S)-4-({isopropyl-[4-methoxy-3-(3-methoxypropane)benzoyl]amino}methyl)pyrrolidin-3-ylmethyl]methylamide (R)-1,2,3,4-tetrahydronaphthalen-2-carboxylic acid,
[(3S,4S)-4-({isopropyl-[4-methoxy-3-(3-methoxypropane)benzoyl]amino}methyl)pyrrolidin-3-ylmethyl]methylamide (S)-1,2,3,4-tetrahydronaphthalen-2-carboxylic acid,
[(3S*,4S*)-4-({isopropyl-[4-methoxy-3-(3-labels is propoxy)benzoyl]amino}methyl)pyrrolidin-3-ylmethyl]methylamide tetrahydropyran-4-carboxylic acid,
N-[(3S,4S)-4-({[2-(1-hydroxycyclohexyl)acetyl]methylamino}methyl)pyrrolidin-3-ylmethyl]-N-isopropyl-4-methoxy-3-(3-methoxypropane)benzamid,
N-isopropyl-4-methoxy-N-(3S,4S)-4-({[2-(4-methoxycyclohexyl)acetyl]methylamino}methyl)pyrrolidin-3-ylmethyl]-3-(3-methoxypropane)benzamid,
N-isopropyl-4-methoxy-N-[(3S,4S)-4-({[2-(4-methoxycyclohexyl)acetyl]methylamino}methyl)pyrrolidin-3-ylmethyl]-3-(3-methoxypropane)benzamid,
[(3S,4S)-4-({isopropyl-[4-methoxy-3-(3-methoxypropane)benzoyl]amino}methyl)pyrrolidin-3-ylmethyl]methylamide 3,4-dihydro-2H-benzo[b][1,4]doxepin-2-carboxylic acid,
N-isopropyl-4-methoxy-N-((3S,4S)-4-{[(CIS-4-methoxycyclohexanone)methylamino]methyl}pyrrolidin-3-ylmethyl)-3-(3-methoxypropane)benzamid,
N-isopropyl-4-methoxy-N-((3S,4S)-4-{[(TRANS-4-methoxycyclohexanone)methylamino]methyl}pyrrolidin-3-ylmethyl)-3-(3-methoxypropane)benzamid,
N-isopropyl-4-methoxy-3-(3-methoxypropane)-N-[(3S,4S)-4-(phenylacetylamino)pyrrolidin-3-ylmethyl]benzamide,
[(3S,4S)-4-({isopropyl-[4-methoxy-3-(3-methoxypropane)benzoyl]amino}methyl)pyrrolidin-3-ylmethyl]amide indan-2-carboxylic acid,
N-{(3S,4S)-4-[((S)-2-cyclohexyl-2-methoxyethylamine)methyl]pyrrolidin-3-ylmethyl}-N-isopropyl-4-methoxy-3-(3-methoxypropane)benzamid,
N-isopropyl-4-methoxy-N-{(3S,4S)-4-[((R)-2-methoxy-2-phenylacetylamino)methyl]pyrrolidin-3-ylmethyl}-3-(3-methoxypropane)benzamid,
N-isopropyl-4-methoxy-N-{(3S,4S)-4-[((S-2-methoxy-2-phenylacetylamino)methyl]pyrrolidin-3-ylmethyl}-3-(3-methoxypropane)benzamid,
N-{(3S,4S)-4-[((R)-2-cyclohexyl-2-methoxyethylamine)methyl]pyrrolidin-3-ylmethyl}-N-isopropyl-4-methoxy-3-(3-methoxypropane)benzamid,
N-{(3S,4S)-4-[(ethylphenethylamine)methyl]pyrrolidin-3-ylmethyl}-N-isopropyl-4-methoxy-3-(3-methoxypropane)benzamid,
N-((3S,4S)-4-{[ethyl-(2-tetrahydropyran-4-ylacetic)amino]methyl}pyrrolidin-3-ylmethyl)-N-isopropyl-4-methoxy-3-(3-methoxypropane)benzamid,
N-{(3S*,4S*)-4-[(cyclobutanemethanamine)methyl]pyrrolidin-3-ylmethyl}-N-isopropyl-4-methoxy-3-(3-methoxypropane)benzamid,
N-((3S*,4S*)-4-{[cyclobutyl-(2-tetrahydropyran-4-ylacetic)amino]methyl}pyrrolidin-3-ylmethyl)-N-isopropyl-4-methoxy-3-(3-methoxypropane)benzamid,
N-isopropyl-N-{(3S*,4S*)-4-[(isopropylbenzylamine)methyl]pyrrolidin-3-ylmethyl}-4-methoxy-3-(3-methoxypropane)benzamid,
N-isopropyl-N-((3S*,4S*)-4-{[isopropyl-(2-tetrahydropyran-4-ylacetic)amino]methyl}pyrrolidin-3-ylmethyl)-4-methoxy-3-(3-methoxypropane)benzamid,
N-{(3S*,4S*)-4-[(cyclopropanecarbonitrile)methyl]pyrrolidin-3-ylmethyl}-N-isopropyl-4-methoxy-3-(3-methoxypropane)benzamid,
N-{(3S*,4S*)-4-[(cyclobutanecarbonitrile)methyl]pyrrolidin-3-ylmethyl}-N-isopropyl-4-methoxy-3-(3-methoxypropane)benzamid,
N-((3S*,4S*)-4-{[isobutyl-(2-tetrahydropyran-4-ylacetic)amino]methyl}pyrrolidin-3-ylmethyl)-N-isopropyl-4-methoxy-3-(3-methoxypropane)benzamid,
N-{(3S*,4S*)-4-[(isobutyrylacetate)methyl]pyrrolidin-3-ylmethyl}-N-out is ropyl-4-methoxy-3-(3-methoxypropane)benzamid,
N-{(3S*,4S*)-4-[(cyclopropylacetylene)methyl]pyrrolidin-3-ylmethyl}-N-isopropyl-4-methoxy-3-(3-methoxypropane)benzamid,
N-((3S*,4S*)-4-{[cyclopropylmethyl-(2-tetrahydropyran-4-ylacetic)amino]methyl}pyrrolidin-3-ylmethyl)-N-isopropyl-4-methoxy-3-(3-methoxypropane)benzamid,
isopropyl-{(3S,4S)-4-[(methylphenylethylamine)methyl]pyrrolidin-3-ylmethyl}amide 1-(3-methoxypropyl)-3-methyl-1H-indole-6-carboxylic acid,
((3S,4S)-4-{[(2-cyclohexylethyl)methylamino]methyl}pyrrolidin-3-ylmethyl)isopropylated 1-(3-methoxypropyl)-3-methyl-1H-indole-6-carboxylic acid,
N-{(3S,4S)-4-[(cyclopropylacetylene)methyl]pyrrolidin-3-ylmethyl}-4-ethyl-N-isopropyl-3-(3-methoxypropane)benzamid,
N-((3S,4S)-4-{[(2-cyclohexylethyl)methylamino]methyl}pyrrolidin-3-ylmethyl)-4-ethyl-N-isopropyl-3-(3-methoxypropane)benzamid,
4-ethyl-N-isopropyl-3-(3-methoxypropane)-N-((3S,4S)-4-{[methyl-(2-tetrahydropyran-4-ylacetic)amino]methyl}pyrrolidin-3-ylmethyl)benzamide,
[(3S,4S)-4-({[4-ethyl-3-(3-methoxypropane)benzoyl]isopropylamino)methyl)pyrrolidin-3-ylmethyl]methylamide tetrahydropyran-4-carboxylic acid,
N-((3S,4S)-4-{[cyclopropyl-(2-tetrahydropyran-4-ylacetic)amino]methyl}pyrrolidin-3-ylmethyl)-4-ethyl-N-isopropyl-3-(3-methoxypropane)benzamid,
cyclopropyl-[(3S,4S)-4-({[4-ethyl-3-(3-methoxypropane)benzoyl]isopropylamino}methyl)pyrrolidin-3-ylmethyl]amide tetrahydropyran-4-carboxylic acid,
N-((3S,4S)-4-{[(3-acety is amino-3-methylbutyryl)cyclopropylamino]methyl}pyrrolidin-3-ylmethyl)-4-ethyl-N-isopropyl-3-(3-methoxypropane)benzamid,
4-ethyl-N-((35,48)-4-{[((S)-2-hydroxy-2-phenylacetyl)methylamino]methyl)pyrrolidin-3-ylmethyl)-N-isopropyl-3-(3-methoxypropane)benzamid,
N-[(3S,4S)-4-({[2-(1-acetylpiperidine-4-yl)acetyl]cyclopropylamino}methyl)pyrrolidin-3-ylmethyl]-4-ethyl-N-isopropyl-3-(3-methoxypropane)benzamid,
N-[(3S,4S)-4-({[2-(1-acetylpiperidine-4-yl)acetyl]methylamino}methyl)pyrrolidin-3-ylmethyl]-4-ethyl-N-isopropyl-3-(3-methoxypropane)benzamid,
4-ethyl-N-((3S,4S)-4-{[((S)-2-hydroxy-4-methylpentanoic)methylamino]methyl}pyrrolidin-3-ylmethyl)-N-isopropyl-3-(3-methoxypropane)benzamid,
4-ethyl-N-((3S,4S)-4-{[((S)-2-hydroxy-3-methylbutyryl)methylamino]methyl}pyrrolidin-3-ylmethyl)-N-isopropyl-3-(3-methoxypropane)benzamid,
[(3S,4S)-4-({[4-ethyl-3-(3-methoxypropane)benzoyl]isopropylamino}methyl)pyrrolidin-3-ylmethyl]amide indan-2-carboxylic acid,
4-ethyl-N-isopropyl-3-(3-methoxypropane)-N-{(3S,4S)-4-[(2-methyl-2-phenylpropionylamino)methyl]pyrrolidin-3-ylmethyl}benzamide,
4-ethyl-N-isopropyl-N-{(3S,4S)-4-[((R)-2-methoxy-2-phenylacetylamino)methyl]pyrrolidin-3-ylmethyl}-3-(3-methoxypropane)benzamid,
4-ethyl-N-[(3S,4S)-4-({[2-(1-hydroxycyclohexyl)acetyl]methylamino}methyl)pyrrolidin-3-ylmethyl]-N-isopropyl-3-(3-methoxypropane)benzamid,
N-[(3S,4S)-4-({[2-(4-aminocyclohexane)acetyl]methylamino}methyl)pyrrolidin-3-ylmethyl]-4-ethyl-N-isopropyl-3-(3-methoxypropane)benzamid,
N-[(3S,4S)-4-({[2-(4-aminocyclohexane)acetyl]methylamino}methyl)pyrrolidin-3-ylmethyl]-4-ethyl-N-isopropyl-3-(3-methoxypropane)benzamid,
[(3S,4S)-4-({[4-ethyl-3-(3-methoxypropane)benzoyl]isopropylamino}methyl)pyrrolidin-3-ylmethyl]methylamide 5-methylpyrazine-2-carboxylic acid,
[(3S,4S)-4-({[4-ethyl-3-(3-methoxypropane)benzoyl]isopropylamino}methyl)pyrrolidin-3-ylmethyl]methylamide (S)-2,3-dihydrobenzo[1,4]dioxin-2-carboxylic acid,
[(3S,4S)-4-({[4-ethyl-3-(3-methoxypropane)benzoyl]isopropylamino}methyl)pyrrolidin-3-ylmethyl]methylamide (R)-2-oxo-1,2,3,4-tetrahydroquinolin-4-carboxylic acid,
[(3S,4S)-4-({[4-ethyl-3-(3-methoxypropane)benzoyl]isopropylamino}methyl)pyrrolidin-3-ylmethyl]methylamide (S)-2-oxo-1,2,3,4-tetrahydroquinolin-4-carboxylic acid,
N-cyclopropyl-N-[(3S,4S)-4-({[4-ethyl-3-(3-methoxypropane)benzoyl]isopropylamino}methyl)pyrrolidin-3-ylmethyl]-N'-methylsuccinimide,
cyclopropyl-[(3S,4S)-4-({[4-ethyl-3-(3-methoxypropane)benzoyl]isopropylamino}methyl)pyrrolidin-3-ylmethyl]amide 5-methylpyrazine-2-carboxylic acid,
cyclopropyl-[(3S,4S)-4-({[4-ethyl-3-(3-methoxypropane)benzoyl]isopropylamino}methyl)pyrrolidin-3-ylmethyl]amide isoxazol-3-carboxylic acid,
N-[(3S,4S)-4-({[2-(4-aminocyclohexane)acetyl]cyclopropylamino}methyl)pyrrolidin-3-ylmethyl]-4-ethyl-N-isopropyl-3-(3-methoxypropane)benzamid,
N-[(3S,4S)-4-({[2-(4-aminocyclohexane)acetyl]cyclopropylamino}methyl)pyrrolidin-3-ylmethyl]-4-ethyl-N-isopropyl-3-(3-methoxypropane)benzamid,
cyclopropyl-[(3S,4S)-4-({[4-ethyl-3-(3-methoxypropane)benzoyl]isopropylamino}methyl)PI is ridin-3-ylmethyl]amide (R)-tetrahydrofuran-3-carboxylic acid,
cyclopropyl-[(3S,4S)-4-({[4-ethyl-3-(3-methoxypropane)benzoyl]isopropylamino}methyl)pyrrolidin-3-ylmethyl]amide (S)-tetrahydrofuran-3-carboxylic acid,
cyclopropyl-[(3S,4S)-4-({[4-ethyl-3-(3-methoxypropane)benzoyl]isopropylamino}methyl)pyrrolidin-3-ylmethyl]amide (R)-tetrahydropyran-3-carboxylic acid,
cyclopropyl-[(3S,4S)-4-({[4-ethyl-3-(3-methoxypropane)benzoyl]isopropylamino}methyl)pyrrolidin-3-ylmethyl]amide (S)-tetrahydropyran-3-carboxylic acid,
N-((3S,4S)-4-{[cyclopropyl-(CIS-4-hydroxycyclohexanone)amino]methyl}pyrrolidin-3-ylmethyl)-4-ethyl-N-isopropyl-3-(3-methoxypropane)benzamid,
N-((3S,4S)-4-{[cyclopropyl-(TRANS-4-hydroxycyclohexanone)amino]methyl}pyrrolidin-3-ylmethyl)-4-ethyl-N-isopropyl-3-(3-methoxypropane)benzamid,
[(3S,4S)-4-({[4-ethyl-3-(3-methoxypropane)benzoyl]isopropylamino}methyl)pyrrolidin-3-ylmethyl]methylamide (S)-tetrahydropyran-3-carboxylic acid,
[(3S,4S)-4-({[4-ethyl-3-(3-methoxypropane)benzoyl]isopropylamino}methyl)pyrrolidin-3-ylmethyl]methylamide (R)-tetrahydropyran-3-carboxylic acid,
N-isopropyl-3-(3-methoxypropane)-4-methyl-N-{(3S,4S)-4-[(methylphenylethylamine)methyl]pyrrolidin-3-ylmethyl}benzamide,
[(3S,4S)-4-({isopropyl-[3-(3-methoxypropane)-4-methylbenzoyl]amino}methyl)pyrrolidin-3-ylmethyl]methylamide tetrahydropyran-4-carboxylic acid,
N-isopropyl-3-(3-methoxypropane)-4-methyl-N-((3S,4S)-4-{[methyl-(2-tetrahydropyran-4-ylacetic)and the Ino]methyl}pyrrolidin-3-ylmethyl)benzamide,
N-((3S,4S)-4-{[cyclopropyl-((S)-2-methoxy-2-phenylacetyl)amino]methyl}pyrrolidin-3-ylmethyl)-N-isopropyl-3-(3-methoxypropane)-4-methylbenzamide,
cyclopropyl-[(3S,4S)-4-({isopropyl-[3-(3-methoxypropane)-4-methylbenzoyl]amino}methyl)pyrrolidin-3-ylmethyl]amide (S)-2,3-dihydrobenzo[1,4]dioxin-2-carboxylic acid,
N-((3S,4S)-4-{[((S)-2-methoxy-2-phenylacetyl)methylamino]methyl}pyrrolidin-3-ylmethyl)-N-isopropyl-3-(3-methoxypropane)-4-methylbenzamide,
[(3S,4S)-4-({isopropyl-[3-(3-methoxypropane)-4-methylbenzoyl]amino}methyl)pyrrolidin-3-ylmethyl]methylamide (S)-2,3-dihydrobenzo[1,4]dioxin-2-carboxylic acid,
N-((3S,4S)-4-{[(3-acetylamino-3-methylbutyryl)cyclopropylamino]methyl}pyrrolidin-3-ylmethyl)-N-isopropyl-3-(3-methoxypropane)-4-methylbenzamide,
N-((3S,4S)-4-{[((S)-2-hydroxy-2-phenylacetyl)methylamino]methyl}pyrrolidin-3-ylmethyl)-N-isopropyl-3-(3-methoxypropane)-4-methylbenzamide,
cyclopropyl-[(3S,4S)-4-({isopropyl-[3-(3-methoxypropane)-4-methylbenzoyl]amino}methyl)pyrrolidin-3-ylmethyl]amide tetrahydropyran-4-carboxylic acid,
N-isopropyl-3-(3-methoxypropane)-4-methyl-N-[(3S,4S)-4-({methyl-[2-(3-oxo-3,4-dihydro-2H-benzo[1,4]oxazin-6-yl)acetyl]amino}methyl)pyrrolidin-3-ylmethyl]benzamide,
N-[(3S,4S)-4-({cyclopropyl-[2-(3-oxo-3,4-dihydro-2H-benzo[1,4]oxazin-6-yl)acetyl]amino}methyl)pyrrolidin-3-ylmethyl]-N-isopropyl-3-(3-methoxypropane)-4-methylbenzamide,
N-((3S,4S)-4-{[cyclopropyl-(2-tetrahydropyran-4-ylacetic)amino]METI the}pyrrolidin-3-ylmethyl)-N-isopropyl-3-(3-methoxypropane)-4-methylbenzamide,
N-((3S,4S)-4-{[((S)-2-cyclohexyl-2-methoxyacetyl)cyclopropylamino]methyl}pyrrolidin-3-ylmethyl)-N-isopropyl-3-(3-methoxypropane)-4-methylbenzamide,
N-((3S,4S)-4-{[((S)-2-cyclohexyl-2-methoxyacetyl)methylamino]methyl}pyrrolidin-3-ylmethyl)-N-isopropyl-3-(3-methoxypropane)-4-methylbenzamide,
N-((3S,4S)-4-{[((S)-2-hydroxy-3-methylbutyryl)methylamino]methyl)pyrrolidin-3-ylmethyl)-N-isopropyl-3-(3-methoxypropane)-4-methylbenzamide,
N-[(3S,4S)-4-({[2-(1-acetylpiperidine-4-yl)acetyl]cyclopropylamino}methyl)pyrrolidin-3-ylmethyl]-N-isopropyl-3-(3-methoxypropane)-4-methylbenzamide,
N-((3S,4S)-4-{[((S)-2-hydroxy-4-methylpentanoic)methylamino]methyl}pyrrolidin-3-ylmethyl)-N-isopropyl-3-(3-methoxypropane)-4-methylbenzamide,
N-((3S,4S)-4-{[(CIS-4-hydroxycyclohexanone)methylamino]methyl}pyrrolidin-3-ylmethyl)-N-isopropyl-3-(3-methoxypropane)-4-methylbenzamide,
N-((3S,4S)-4-{[((R)-3-hydroxy-3-phenylpropionyl)methylamino]methyl}pyrrolidin-3-ylmethyl)-N-isopropyl-3-(3-methoxypropane)-4-methylbenzamide,
N-((3S,4S)-4-{[((S)-3-hydroxy-3-phenylpropionyl)methylamino]methyl}pyrrolidin-3-ylmethyl)-N-isopropyl-3-(3-methoxypropane)-4-methylbenzamide,
N-[(3S,4S)-4-({[2-(1-acetylpiperidine-4-yl)acetyl]methylamino}methyl)pyrrolidin-3-ylmethyl]-N-isopropyl-3-(3-methoxypropane)-4-methylbenzamide,
N-((3S,4S)-4-{[cyclopropyl-(CIS-4-hydroxycyclohexanone)amino]methyl}pyrrolidin-3-ylmethyl)-N-isopropyl-3-(3-methoxypropane)-4-methylbenzamide,
N-((3S,4S)-4-{(S)-2-hydroxy-3-phenylpropionyl)methylamino]methyl}pyrrolidin-3-ylmethyl)-N-isopropyl-3-(3-methoxypropane)-4-methylbenzamide,
N-((3S,4S)-4-{[(2-furan-2-ylacetic)methylamino]methyl}pyrrolidin-3-ylmethyl)-N-isopropyl-3-(3-methoxypropane)-4-methylbenzamide,
N-((3S,4S)-4-{[cyclopropyl-((S)-2-hydroxy-4-methylpentanoic)amino]methyl}pyrrolidin-3-ylmethyl)-N-isopropyl-3-(3-methoxypropane)-4-methylbenzamide,
[(3S,4S)-4-({isopropyl-[3-(3-methoxypropane)-4-methylbenzoyl]amino}methyl)pyrrolidin-3-ylmethyl]amide indan-2-carboxylic acid,
N-isopropyl-3-(3-methoxypropane)-4-methyl-N-{(3S,4S)-4-[(2-methyl-2-phenylpropionylamino)methyl]pyrrolidin-3-ylmethyl}benzamide,
N-isopropyl-3-(3-methoxypropane)-4-methyl-N-{(3S,4S)-4-[(2-tetrahydropyran-4-ylacetamide)methyl]pyrrolidin-3-ylmethyl}benzamide,
[(3S,4S)-4-({isopropyl-[3-(3-methoxypropane)-4-methylbenzoyl]amino}methyl)pyrrolidin-3-ylmethyl]amide (S)-2,3-dihydrobenzo[1,4]dioxin-2-carboxylic acid,
N-isopropyl-3-(3-methoxypropane)-4-methyl-N-((3S,4S)-4-{[methyl-((R)-2-tetrahydropyran-2-ylacetic)amino]methyl}pyrrolidin-3-ylmethyl)benzamide,
N-isopropyl-3-(3-methoxypropane)-4-methyl-N-((3S,4S)-4-{[methyl-((S)-2-tetrahydropyran-2-ylacetic)amino]methyl}pyrrolidin-3-ylmethyl)benzamide,
N-((3S,4S)-4-{[cyclopropyl-((R)-2-tetrahydrofuran-2-ylacetic)amino]methyl}pyrrolidin-3-ylmethyl)-N-isopropyl-3-(3-methoxypropane)-4-methylbenzamide,
N-((3S,4S)-4-{[cyclopropyl-((S)-2-tetrahydrofuran-2-ylacetic)amino]methyl}pyrrolidin-3-ylmethyl)-N-isopropyl-3-(3-methoxypropane)-4-methylbenzamide,
N-isopropyl-N-((3S,4S)-4-{[(CIS-4-methoxyclor cancerboy)methylamino]methyl}pyrrolidin-3-ylmethyl)-3-(3-methoxypropane)-4-methylbenzamide,
N-isopropyl-N-((3S,4S)-4-{[(TRANS-4-methoxycyclohexanone)methylamino]methyl}pyrrolidin-3-ylmethyl)-3-(3-methoxypropane)-4-methylbenzamide,
N-isopropyl-N-((3S,4S)-4-{[(CIS-4-methoxycyclohexanone)amino]methyl}pyrrolidin-3-ylmethyl)-3-(3-methoxypropane)-4-methylbenzamide,
N-isopropyl-N-((3S,4S)-4-{[(TRANS-4-methoxycyclohexanone)amino]methyl}pyrrolidin-3-ylmethyl)-3-(3-methoxypropane)-4-methylbenzamide,
isopropyl-{(3S,4S)-4-[(methylphenylethylamine)methyl]pyrrolidin-3-ylmethyl}amide 1-(3-methoxypropyl)-1H-indole-6-carboxylic acid,
N-cyclopropyl-N-{(3S,4S)-4-[(cyclopropylacetylene)methyl]pyrrolidin-3-ylmethyl}-4-methoxy-3-(3-methoxypropane)benzamid,
benzyl ether cyclopropyl-[(3S,4S)-4-({cyclopropyl-[4-methoxy-3-(3-methoxypropane)benzoyl]amino}methyl)pyrrolidin-3-ylmethyl]carbamino acid,
isobutyl ether cyclopropyl-[(3S,4S)-4-({cyclopropyl-[4-methoxy-3-(3-methoxypropane)benzoyl]amino}methyl)pyrrolidin-3-ylmethyl]carbamino acid,
tetrahydropyran-4-silt ether cyclopropyl-[(3S,4S)-4-({cyclopropyl-[4-methoxy-3-(3-methoxypropane)benzoyl]amino}methyl)pyrrolidin-3-ylmethyl]carbamino acid,
benzyl ether cyclopropyl-[(3S*,4S*)-4-({isopropyl-[4-methoxy-3-(3-methoxypropane)benzoyl]amino}methyl)pyrrolidin-3-ylmethyl]carbamino acid,
benzyl ether cyclopropyl-[(3S,4S)-4-({isopropyl-[4-methoxy-3-(3-methoxypropane)benzoyl]amino}METI is)pyrrolidin-3-ylmethyl]carbamino acid,
isobutyl ether cyclopropyl-[(3S*,4S*)-4-({isopropyl-[4-methoxy-3-(3-methoxypropane)benzoyl]amino}methyl)pyrrolidin-3-ylmethyl]carbamino acid,
pyridine-4-ymetray ether cyclopropyl-[(3S*,4S*)-4-({isopropyl-[4-methoxy-3-(3-methoxypropane)benzoyl]amino}methyl)pyrrolidin-3-ylmethyl]carbamino acid,
1 methylpiperidin-4-ymetray ether cyclopropyl-[(3S*,4S*)-4-({isopropyl-[4-methoxy-3-(3-methoxypropane)benzoyl]amino}methyl)pyrrolidin-3-ylmethyl]carbamino acid,
2-methoxyethylamine ether cyclopropyl-[(3S*,4S*)-4-({isopropyl-[4-methoxy-3-(3-methoxypropane)benzoyl]amino}methyl)pyrrolidin-3-ylmethyl]carbamino acid,
tetrahydropyran-4-ymetray ether cyclopropyl-[(3S*,4S*)-4-({isopropyl-[4-methoxy-3-(3-methoxypropane)benzoyl]amino}methyl)pyrrolidin-3-ylmethyl]carbamino acid,
2,2-dimethylpropionic ether cyclopropyl-[(3S*,4S*)-4-({isopropyl-[4-methoxy-3-(3-methoxypropane)benzoyl]amino}methyl)pyrrolidin-3-ylmethyl]carbamino acid,
1-methylcyclopropyl ether cyclopropyl-[(3S*,4S*)-4-({isopropyl-[4-methoxy-3-(3-methoxypropane)benzoyl]amino}methyl)pyrrolidin-3-ylmethyl]carbamino acid,
2-acetylamino-2-methylpropionyl ether cyclopropyl-[(3S*,4S*)-4-({isopropyl-[4-methoxy-3-(3-methoxypropane)benzoyl]amino}methyl)pyrrolidin-3-ylmethyl]carbamino acid,
phenyl ether cyclopropyl-[(3S*,4S*)-4-({isopropyl-[4-methoxy-3-(3-methoxyp is poxi)benzoyl]amino}methyl)pyrrolidin-3-ylmethyl]carbamino acid,
2-methyl-2-methylcarbamoylmethyl ether cyclopropyl-[(3S*,4S*)-4-({isopropyl-[4-methoxy-3-(3-methoxypropane)benzoyl]amino}methyl)pyrrolidin-3-ylmethyl]carbamino acid,
1-acetaminophenrelatively ether cyclopropyl-[(3S*,4S*)-4-({isopropyl-[4-methoxy-3-(3-methoxypropane)benzoyl]amino}methyl)pyrrolidin-3-ylmethyl]carbamino acid,
1-acetylpiperidine-4-ymetray ether cyclopropyl-[(3S*,4S*)-4-({isopropyl-[4-methoxy-3-(3-methoxypropane)benzoyl]amino}methyl)pyrrolidin-3-ylmethyl]carbamino acid,
5-methylisoxazol-3-ymetray ether cyclopropyl-[(3S*,4S*)-4-({isopropyl-[4-methoxy-3-(3-methoxypropane)benzoyl]amino}methyl)pyrrolidin-3-ylmethyl]carbamino acid,
naphthalene-1-silt ether cyclopropyl-[(3S*,4S*)-4-({isopropyl-[4-methoxy-3-(3-methoxypropane)benzoyl]amino}methyl)pyrrolidin-3-ylmethyl]carbamino acid,
cyclopropylmethoxy ether cyclopropyl-[(3S,4S)-4-({isopropyl-[4-methoxy-3-(3-methoxypropane)benzoyl]amino}methyl)pyrrolidin-3-ylmethyl]carbamino acid,
isobutyl ether cyclopropyl-[(3S,4S)-4-({isopropyl-[4-methoxy-3-(3-methoxypropane)benzoyl]amino}methyl)pyrrolidin-3-ylmethyl]carbamino acid,
4-methoxybenzyloxy ether cyclopropyl-[(3S,4S)-4-({isopropyl-[4-methoxy-3-(3-methoxypropane)benzoyl]amino}methyl)pyrrolidin-3-ylmethyl]carbamino acid,
cyclohexyloxy ether cyclopropyl-[(3S,4S)-4-({isopropyl-[4-methoxy-3-(methoxypropane)benzoyl]amino}methyl)pyrrolidin-3-ylmethyl]carbamino acid,
naphthalene-2-silt ether cyclopropyl-[(3S,4S)-4-({isopropyl-[4-methoxy-3-(3-methoxypropane)benzoyl]amino}methyl)pyrrolidin-3-ylmethyl]carbamino acid,
tetrahydropyran-4-silt ether cyclopropyl-[(3S,4S)-4-({isopropyl-[4-methoxy-3-(3-methoxypropane)benzoyl]amino}methyl)pyrrolidin-3-ylmethyl]carbamino acid,
5-methyl-[1,3]dioxane-5-ymetray ether cyclopropyl-[(3S,4S)-4-({isopropyl-[4-methoxy-3-(3-methoxypropane)benzoyl]amino}methyl)pyrrolidin-3-ylmethyl]carbamino acid,
3-(2-oxo-pyrrolidin-1-yl)phenyl ether cyclopropyl-[(3S,4S)-4-({isopropyl-[4-methoxy-3-(3-methoxypropane)benzoyl]amino}methyl)pyrrolidin-3-ylmethyl]carbamino acid,
3-morpholine-4-ilenylady ether cyclopropyl-[(3S,4S)-4-({isopropyl-[4-methoxy-3-(3-methoxypropane)benzoyl]amino}methyl)pyrrolidin-3-ylmethyl]carbamino acid,
(R)-1-(tetrahydrofuran-2-yl)methyl ether cyclopropyl-[(3S,4S)-4-({isopropyl-[4-methoxy-3-(3-methoxypropane)benzoyl]amino}methyl)pyrrolidin-3-ylmethyl]carbamino acid,
(R)-1-phenylpropylamine ether cyclopropyl-[(3S,4S)-4-({isopropyl-[4-methoxy-3-(3-methoxypropane)benzoyl]amino}methyl)pyrrolidin-3-ylmethyl]carbamino acid,
(R)-1-phenethyl ether cyclopropyl-[(3S,4S)-4-({isopropyl-[4-methoxy-3-(3-methoxypropane)benzoyl]amino}methyl)pyrrolidin-3-ylmethyl]carbamino acid,
phenyl ether cyclopropyl-[(3S,4S)-4-({isopropyl-[4-methoxy-3-(3-methoxypropan the si)benzoyl]amino}methyl)pyrrolidin-3-ylmethyl]carbamino acid,
2-methoxyphenoxy ether cyclopropyl-[(3S,4S)-4-({isopropyl-[4-methoxy-3-(3-methoxypropane)benzoyl]amino}methyl)pyrrolidin-3-ylmethyl]carbamino acid,
3-methoxy-3-methylbutanoyl ether cyclopropyl-[(3S,4S)-4-({isopropyl-[4-methoxy-3-(3-methoxypropane)benzoyl]amino}methyl)pyrrolidin-3-ylmethyl]carbamino acid,
(R)-(tetrahydrofuran-3-yl)ether cyclopropyl-[(3S,4S)-4-({isopropyl-[4-methoxy-3-(3-methoxypropane)benzoyl]amino}methyl)pyrrolidin-3-ylmethyl]carbamino acid,
(S)-(tetrahydrofuran-3-yl)ether cyclopropyl-[(3S,4S)-4-({isopropyl-[4-methoxy-3-(3-methoxypropane)benzoyl]amino}methyl)pyrrolidin-3-ylmethyl]carbamino acid,
3-methoxy-3-methylbutanoyl ester [(3S,4S)-4-({isopropyl-[4-methoxy-3-(3-methoxypropane)benzoyl]amino}methyl)pyrrolidin-3-ylmethyl]methylcarbamate acid,
tetrahydropyran-4-silt ester [(3S,4S)-4-({isopropyl-[4-methoxy-3-(3-methoxypropane)benzoyl]amino}methyl)pyrrolidin-3-ylmethyl]methylcarbamate acid,
tetrahydropyran-4-silt ether cyclopropyl-[(3S,4S)-4-({isopropyl-[3-(3-methoxypropane)-4-methylbenzoyl]amino}methyl)pyrrolidin-3-ylmethyl]carbamino acid,
(S)-(tetrahydrofuran-3-yl)ether cyclopropyl-[(3S,4S)-4-({isopropyl-[3-(3-methoxypropane)-4-methylbenzoyl]amino}methyl)pyrrolidin-3-ylmethyl]carbamino acid,
tetrahydropyran-4-silt ester [(3S,4S)-4-({isopropyl-[3-(3-methoxypropane)-4-methylbenzoyl]amino}methyl)pirol the Dean-3-ylmethyl]methylcarbamate acid,
(S)-(tetrahydrofuran-3-yl)ester [(3S,4S)-4-({isopropyl-[3-(3-methoxypropane)-4-methylbenzoyl]amino}methyl)pyrrolidin-3-ylmethyl]methylcarbamate acid,
3-methoxy-3-methylbutanoyl ester [(3S,4S)-4-({isopropyl-[3-(3-methoxypropane)-4-methylbenzoyl]amino}methyl)pyrrolidin-3-ylmethyl]methylcarbamate acid,
3-methoxy-3-methylbutanoyl ether cyclopropyl-[(3S,4S)-4-({isopropyl-[3-(3-methoxypropane)-4-methylbenzoyl]amino}methyl)pyrrolidin-3-ylmethyl]carbamino acid,
4-methoxybenzyloxy ester[(3S,4S)-4-({isopropyl-[3-(3-methoxypropane)-4-methylbenzoyl]amino}methyl)pyrrolidin-3-ylmethyl]methylcarbamate acid,
(R)-1-(tetrahydrofuran-2-yl)methyl ester [(3S,4S)-4-({isopropyl-[3-(3-methoxypropane)-4-methylbenzoyl]amino}methyl)pyrrolidin-3-ylmethyl]methylcarbamate acid,
4-methoxybenzyloxy ether cyclopropyl-[(3S,4S)-4-({isopropyl-[3-(3-methoxypropane)-4-methylbenzoyl]amino}methyl)pyrrolidin-3-ylmethyl]carbamino acid,
(R)-1-(tetrahydrofuran-2-yl)methyl ether cyclopropyl-[(3S,4S)-4-({isopropyl-[3-(3-methoxypropane)-4-methylbenzoyl]amino}methyl)pyrrolidin-3-ylmethyl]carbamino acid,
5-methyl-[1,3]dioxane-5-ymetray ester [(3S,4S)-4-({isopropyl-[3-(3-methoxypropane)-4-methylbenzoyl]amino}methyl)pyrrolidin-3-ylmethyl]methylcarbamate acid,
5-methylisoxazol-3-ymetray ether cyclopropyl-[(3S,4S)-4-({isopropyl-[3-(3-methoxypropane)-4-methylbenzoyl]amino}methylpyridin-3-ylmethyl]carbamino acid,
5-methylisoxazol-3-ymetray ester [(3S,4S)-4-({isopropyl-[3-(3-methoxypropane)-4-methylbenzoyl]amino}methyl)pyrrolidin-3-ylmethyl]methylcarbamate acid,
benzyl ether cyclopropyl-[(3S,4S)-4-({[4-ethyl-3-(3-methoxypropane)benzoyl]isopropylamino}methyl)pyrrolidin-3-ylmethyl]carbamino acid,
tetrahydropyran-4-silt ether cyclopropyl-[(3S,4S)-4-({[4-ethyl-3-(3-methoxypropane)benzoyl]isopropylamino}methyl)pyrrolidin-3-ylmethyl]carbamino acid,
4-methoxybenzyloxy ether cyclopropyl-[(3S,4S)-4-({[4-ethyl-3-(3-methoxypropane)benzoyl]isopropylamino}methyl)pyrrolidin-3-ylmethyl]carbamino acid,
tetrahydropyran-4-silt ester [(3S,4S)-4-({[4-ethyl-3-(3-methoxypropane)benzoyl]isopropylamino}methyl)pyrrolidin-3-ylmethyl]methylcarbamate acid,
(R)-1-(tetrahydrofuran-2-yl)methyl ester[(3S,4S)-4-({[4-ethyl-3-(3-methoxypropane)benzoyl]isopropylamino}methyl)pyrrolidin-3-ylmethyl]methylcarbamate acid,
(S)-(tetrahydrofuran-3-yl)ester [(3S,4S)-4-({[4-ethyl-3-(3-methoxypropane)benzoyl]isopropylamino}methyl)pyrrolidin-3-ylmethyl]methylcarbamate acid,
5-methyl-[1,3]dioxane-5-ymetray ester[(3S,4S)-4-({[4-ethyl-3-(3-methoxypropane)benzoyl]isopropylamino}methyl)pyrrolidin-3-ylmethyl]methylcarbamate acid,
3-methoxy-3-methylbutanoyl ester [(3S,4S)-4-({[4-ethyl-3-(3-methoxypropane)benzoyl]isopropylamino}methyl)pyrrolidin-3-ylmethyl]methylcarbamate sour is s,
benzyl ether cyclopropyl-[(3S,4S)-4-({isopropyl-[1-(3-methoxypropyl)-3-methyl-1H-indole-6-carbonyl]amino}methyl)pyrrolidin-3-ylmethyl]carbamino acid,
isobutyl ether cyclopropyl-[(3S,4S)-4-({isopropyl-[1-(3-methoxypropyl)-3-methyl-1H-indole-6-carbonyl]amino}methyl)pyrrolidin-3-ylmethyl]carbamino acid,
tetrahydropyran-4-silt ether cyclopropyl-[(3S,4S)-4-({isopropyl-[1-(3-methoxypropyl)-3-methyl-1H-indole-6-carbonyl]amino}methyl)pyrrolidin-3-ylmethyl]carbamino acid,
(3S*,4S*)-4-({isopropyl-[4-methoxy-3-(3-methoxypropane)benzoyl]amino}methyl)pyrrolidin-3-ymetray ether benzylmethylamine acid,
(3S,4S)-4-({isopropyl-[4-methoxy-3-(3-methoxypropane)benzoyl]amino}methyl)pyrrolidin-3-ymetray ether diisobutylaluminum acid,
(3S,4S)-4-({isopropyl-[4-methoxy-3-(3-methoxypropane)benzoyl]amino}methyl)pyrrolidin-3-ymetray ether benzylisoquinolines acid,
(3S,4S)-4-({isopropyl-[4-methoxy-3-(3-methoxypropane)benzoyl]amino}methyl)pyrrolidin-3-ymetray ether isobutylmethylxanthine acid,
(3S,4S)-4-({isopropyl-[4-methoxy-3-(3-methoxypropane)benzoyl]amino}methyl)pyrrolidin-3-ymetray ether cyclopropyl-(tetrahydropyran-4-ylmethyl)carbamino acid,
(3S,4S)-4-({isopropyl-[4-methoxy-3-(3-methoxypropane)benzoyl]amino}methyl)pyrrolidin-3-ymetray ether cyclopropyl-(tetrahydropyran-4-yl)carbamino acid, (3S,4S)-4-({[4-ethyl-3-(3-methoxypropane)benzoyl]isopropylamino}methyl)pyrrolidin-3-ymetray ether cyclohexyldimethylamine acid,
(3S,4S)-4-({[4-ethyl-3-(3-methoxypropane)benzoyl]isopropylamino}methyl)pyrrolidin-3-ymetray ether benzylisoquinolines acid,
(3S,4S)-4-({[4-ethyl-3-(3-methoxypropane)benzoyl]isopropylamino}methyl)pyrrolidin-3-ymetray ether cyclopropyl(tetrahydropyran-4-ylmethyl)carbamino acid,
(3S,4S)-4-({[4-ethyl-3-(3-methoxypropane)benzoyl]isopropylamino)methyl)pyrrolidin-3-ymetray ether cyclopropyl(tetrahydropyran-3-ylmethyl)carbamino acid,
(3S,4S)-4-({[4-ethyl-3-(3-methoxypropane)benzoyl]isopropylamino)methyl)pyrrolidin-3-ymetray ether cyclopropyl(tetrahydropyran-4-yl)carbamino acid,
(3S,4S)-4-({[4-ethyl-3-(3-methoxypropane)benzoyl]isopropylamino}methyl)pyrrolidin-3-ymetray ether cyclopropyl(tetrahydropyran-2-ylmethyl)carbamino acid,
(3S,4S)-4-({isopropyl-[1-(3-methoxypropyl)-3-methyl-1H-indole-6-carbonyl]amino}methyl)pyrrolidin-3-ymetray ether cyclopropyl(tetrahydropyran-4-yl)carbamino acid,
(3S,4S)-4-({isopropyl-[4-methoxy-3-(3-methoxypropane)benzoyl]amino}methyl)pyrrolidin-3-ymetray ester ((R)-1-phenylpropyl)carbamino acid,
N-(3S*,4S*)-4-(1-cyclopropyl-3-furan-2-eletronically)pyrrolidin-3-ylmethyl]-N-isopropyl-4-methoxy-3-(3-methoxypropane)benzamid, N-[(3S,4S)-4-(1-cyclopropyl-3-furan-2-eletronically)pyrrolidin-3-ylmethyl]-N-isopropyl-4-methoxy-3-(3-methoxypropane)benzamid,
N-[(3S*,4S*)-4-(3-(4-methoxybenzyl-1-cyclopropylmethyl)pyrrolidin-3-ylmethyl]-N-isopropyl-4-methoxy-3-(3-methoxypropane)benzamid,
N-[(3S*,4S*)-4-(3-(4-chlorbenzyl-1-cyclopropylmethyl)pyrrolidin-3-ylmethyl]-N-isopropyl-4-methoxy-3-(3-methoxypropane)benzamid,
N-[(3S*,4S*)-4-(3-(4-terbisil-1-cyclopropylmethyl)pyrrolidin-3-ylmethyl]-N-isopropyl-4-methoxy-3-(3-methoxypropane)benzamid,
N-[(3S*,4S*)-4-(3-cyclohexylmethyl-1-cyclopropylmethyl)pyrrolidin-3-ylmethyl]-N-isopropyl-4-methoxy-3-(3-methoxypropane)benzamid,
N-{(3S*,4S*)-4-[1-cyclopropyl-3-(tetrahydropyran-4-ylmethyl)freedomites]pyrrolidin-3-ylmethyl}-N-isopropyl-4-methoxy-3-(3-methoxypropane)benzamid,
N-[(3S*,4S*)-4-(1-cyclopropyl-3-penetrometer)pyrrolidin-3-ylmethyl]-N-isopropyl-4-methoxy-3-(3-methoxypropane)benzamid,
N-[(3S*,4S*)-4-(1-cyclopropyl-3,3-diphenylpropyl)pyrrolidin-3-ylmethyl]-N-isopropyl-4-methoxy-3-(3-methoxypropane)benzamid,
N-[(3S*,4S*)-4-(1-cyclopropyl-3,3-diisopropylaminomethyl)pyrrolidin-3-ylmethyl]-N-isopropyl-4-methoxy-3-(3-methoxypropane)benzamid,
N-[(3S*,4S*)-4-(3-benzyl-1-cyclopropyl-3-methyluridine)pyrrolidin-3-ylmethyl]-N-isopropyl-4-methoxy-3-(3-methoxypropane)benzamid,
N-[(3S*,4S*)-4-(3-benzyl-1-cyclopropyl-3-ailuridae)pyrrolidin-3-ylmethyl]-N-isopro the Il-4-methoxy-3-(3-methoxypropane)benzamid,
N-[(3S,4S)-4-(3-benzyl-1-cyclopropyl-3-ailuridae)pyrrolidin-3-ylmethyl]-N-isopropyl-4-methoxy-3-(3-methoxypropane)benzamid,
N-[(3S*,4S*)-4-(3-benzyl-1,3-dicyclopentadienyl)pyrrolidin-3-ylmethyl]-N-isopropyl-4-methoxy-3-(3-methoxypropane)benzamid,
N-[(3S*,4S*)-4-(1-cyclopropyl-3-phenylurazole)pyrrolidin-3-ylmethyl]-N-isopropyl-4-methoxy-3-(3-methoxypropane)benzamid,
N-[(3S*,4S*)-4-(3-benzhydryl-1-cyclopropylmethyl)pyrrolidin-3-ylmethyl]-N-isopropyl-4-methoxy-3-(3-methoxypropane)benzamid,
N-[(3S,4S)-4-(3-benzyl-1-cyclopropylmethyl)pyrrolidin-3-ylmethyl]-N-isopropyl-4-methoxy-3-(3-methoxypropane)benzamid,
N-[(3S*,4S*)-4-(1,3-dicyclopropyl-3-phenylurazole)pyrrolidin-3-helmeted]-N-isopropyl-4-methoxy-3-(3-methoxypropane)benzamid,
N-[(3S*,4S*)-4-(3-cyclohexyl-1-cyclopropylethyl)-pyrrolidin-3-ylmethyl]-N-isopropyl-4-methoxy-3-(3-methoxypropane)benzamid,
N-[(3S*,4S*)-4-(1-cyclopropyl-3-naphthalene-1-jureidini)-pyrrolidin-3-ylmethyl]-N-isopropyl-4-methoxy-3-(3-methoxypropane)benzamid,
N-[(3S,4S)-4-(1-cyclopropyl-3-naphthalene-2-jureidini)-pyrrolidin-3-ylmethyl]-N-isopropyl-4-methoxy-3-(3-methoxypropane)benzamid,
N-{(3S,4S)-4-[1-cyclopropyl-3-((R)-1-phenylpropyl)freedomites]pyrrolidin-3-ylmethyl}-N-isopropyl-4-methoxy-3-(3-methoxypropane)benzamid,
N-[(3S,4S)-4-(1-cyclopropyl-3-isobutyl-3-methyluridine)pyrrolidin-3-ylmethyl]-N-isopropyl-4-methoxy-3-(3-methoxypropane)b is same,
N-{(3S,4S)-4-[1-cyclopropyl-3-((S)-1-phenylpropyl)freedomites]pyrrolidin-3-ylmethyl}-N-isopropyl-4-methoxy-3-(3-methoxypropane)benzamid,
cyclopropyl-[(3S,4S)-4-({isopropyl-[4-methoxy-3-(3-methoxypropane)benzoyl]amino}methyl)pyrrolidin-3-ylmethyl]amide (R)-3-phenylpyrrolidine-1-carboxylic acid,
4-ethyl-3-(3-hydroxypropoxy)-N-isopropyl-N-{(3S,4S)-4-[(methylphenylethylamine)methyl]pyrrolidin-3-ylmethyl}benzamide,
N-{(3S,4S)-4-[(cyclopropylacetylene)methyl]pyrrolidin-3-ylmethyl}-3-(3-hydroxypropoxy)-N-isopropyl-4-methoxybenzamide,
N-{(3S*,4S*)-4-[(cyclopropylacetylene)methyl]pyrrolidin-3-ylmethyl}-N-isopropyl-4-methoxy-3-(4-methoxybutyl)benzamid,
N-{(3S*,4S*)-4-[(cyclopropylacetylene)methyl]pyrrolidin-3-ylmethyl}-4-deformity-N-isopropyl-3-(3-methoxypropane)benzamid,
{(3S*,4S*)-4-[(cyclopropylacetylene)methyl]pyrrolidin-3-ylmethyl}isopropylamino 8-(3-methoxypropane)-2,3-dihydrobenzo[1,4]dioxin-6-carboxylic acid,
N-{(3S*,4S*)-4-[(cyclopropylacetylene)methyl]pyrrolidin-3-ylmethyl}-N-isopropyl-4-methoxy-5-(3-methoxypropane)-2-methylbenzamide,
2-chloro-N-{(3S*,4S*)-4-[(cyclopropylacetylene)-methyl]pyrrolidin-3-ylmethyl}-N-isopropyl-4-methoxy-5-(3-methoxypropane)benzamid,
3-chloro-N-{(3S*,4S*)-4-[(cyclopropylacetylene)-methyl]pyrrolidin-3-ylmethyl}-N-isopropyl-5-(3-methoxypropane)benzamid,
4-chloro-N-{(3S*,4S*)-4-[(cyclopropylacetylene)-methyl]pyro is one-3-ylmethyl}-N-isopropyl-3-(3-methoxypropane)benzamid,
4-tert-butyl-N-isopropyl-3-(3-methoxypropane)-N-{(3S,4S)-4-[(methylphenylethylamine)methyl]pyrrolidin-3-ylmethyl}benzamide,
N-isopropyl-4-methoxy-3-(2-methoxyethoxymethyl)-N-{(3S,4S)-4-[(methylphenylethylamine)methyl]pyrrolidin-3-ylmethyl}benzamide,
N-isopropyl-3-(2-methoxyethoxymethyl)-N-{(3S,4S)-4-[(methylphenylethylamine)methyl]pyrrolidin-3-ylmethyl}-4-cryptomaterial,
N-isopropyl-4-methoxy-N-{(3S,4S)-4-[(methylphenylethylamine)methyl]pyrrolidin-3-ylmethyl}-3-(3,3,3-cryptocracy)benzamid,
N-isopropyl-4-methoxy-N-{(3S,4S)-4-[(methylphenylethylamine)methyl]pyrrolidin-3-ylmethyl}-3-(4,4,4-triptoreline)benzamid,
N-{(3S,4S)-4-[(cyclopropylacetylene)methyl]pyrrolidin-3-emetel}-N-isopropyl-4-methoxy-3-(3-cryptometrics)benzamid,
N-{(3S,4S)-4-[(cyclopropylacetylene)methyl]pyrrolidin-3-ylmethyl}-4-ethyl-N-isopropyl-3-(3-cryptometrics)benzamid,
N-isopropyl-4-methoxy-3-(5-methylisoxazol-3-ylethoxy)-N-{(3S,4S)-4-[(methylphenylethylamine)methyl]pyrrolidin-3-ylmethyl}benzamide,
N-{(3S,4S)-4-[(cyclopropylacetylene)methyl]pyrrolidin-3-ylmethyl}-N-isopropyl-3-(2-methoxyethoxymethyl)-4-cryptomaterial,
3-(2-ethoxyethoxy)-N-isopropyl-4-methoxy-N-{(3S,4S)-4-[(methylphenylethylamine)methyl]pyrrolidin-3-ylmethyl}benzamide,
N-[(3S*,4S*)-4-({cyclopropyl-[2-(4-methoxyphenyl)acetyl]amino}methyl)pyrrolidin-3-ylmethyl]-N-isopropyl-4-methoxy-3-(3-methoxypropane)benzamid, and
or its pharmaceutically acceptable salt.

5. The compound according to claim 1 of the formula
or
or its pharmaceutically acceptable salt.

6. Pharmaceutical composition having inhibitory activity against renin, comprising the compound of the formula I according to claim 1 or its pharmaceutically acceptable salt and pharmaceutically acceptable material media.

7. A method of treating hypertension, comprising the introduction of a warm-blooded animal in need of such treatment, a pharmaceutically effective amount of the compounds of formula I according to claim 1 or its pharmaceutically acceptable salt.



 

Same patents:

FIELD: medicine, pharmaceutics.

SUBSTANCE: claimed invention relates to oxazole compound represented by formula (1) and its pharmaceutically acceptable salts. In formula (1) R1 represents phenyl group, which can contain one or two substituents, selected from the following groups (1-1)-(1-11): (1-1) hydroxy groups, (1-2) unsubstituted or halogen-substituted lower alkoxy groups, (1-3) lower alkenyloxy-groups, (1-4) lower alkinyloxy groups, (1-5) cycloC3-8alkyl (lower) alkoxy groups, (1-6) cycloC3-8alkyloxy groups, (1-7) cycloC3-8alkenyloxy groups, (1-8) dihydroindenyloxy groups, (1-9) hydroxyl-(lower)ankoxy groups, (1-10) oxiranyl(lower)alkoxy groups, and (1-11) phenyl(lower)-alkoxy groups; R2 represents phenyl group or heterocyclyl group, selected from pyridine, pyrasine, isoquinoline, pyrrolidine, piperazine, morpholine, each of which can contain one or two substituents, selected from the following groups (2-1)-(2-10):(2-1) hydroxy groups, (2-2) unsubstituted or halogen-substituted lower alkoxy groups, (2-3) unsubstituted or halogen-substituted lower alkyl groups, (2-4) lower alkenyloxy groups, (2-5) halogen atoms, (2-6) lower alkanoyl groups, (2-7) lower alkylthio groups, (2-8) lower alkylsulphonyl groups, (2-9) oxo groups and (2-10) groups lower alkoxy-lower alkoxy; and W represents bivalent group represented by formula (i) or (ii): formula (i) -Y -A -, formula (ii) -Y2-C(=O)-, where A1 represents lower alkenylene group or lower alkylene group, which can contain one substitutent, selected from group, consisting from hydroxy group and lower alkoxicarbonyl group, Y1 represents simple bond, -C(=O)-, -C(=O)-N(R3)-, -N(R4)-C(=O)-, -S(O)m-NH- or -S(O)n-, where R3 and R4, each independently, represent a hydrogen atom or lower alkyl group, and m and n, each independently, represent integer, which has value 2, and Y represents pyperazine-diyl group, or bivalent group, represented by formula (iii) or (iv): formula (iii) -C (=O)-A2-N(R5)-, formula (iv) A3-N(R6)-, where A2 and A3, each independently, represent lower alkylene group, and R5 and R6, each independently, represent a hydrogen atom. Invention also relates to pharmaceutical composition, containing the invention compound as an active ingredient, to pharmaceutical composition for treatment or prevention of atopic dermatitis, which includes the invention compound, to application of the compound as medication, to application of the compound as phosphodiesterase 4 inhibitor and/or as inhibitor of production of tumour necrosis factor α and to method of treatment or prevention of diseases, mediated by phosphodiesterase 4 or mediated by tumour necrosis factor α, including introduction of efficient dose of the compound.

EFFECT: creation of pharmaceutical composition for treatment or prevention of diseases mediated by phosphodiesterase 4 or mediated by tumour necrosis factor, as well as for treatment or prevention of atopic dermatitis.

12 cl, 42 tbl, 486 ex

FIELD: chemistry.

SUBSTANCE: invention relates to (3-trifluromethylphenyl)amide 6-(6-hydroxymethylpyrimidin-4-yloxy)naphthalene-1-carboxylic acid or tautomer or salt thereof. The invention also relates to a pharmaceutical composition which has protein kinase inhibiting activity, based on the said compound and use of the said compound to prepare pharmaceutical compositions for use in treating protein kinase dependent diseases, preferably proliferative diseases, particularly tumorous diseases.

EFFECT: improved properties of compounds.

6 cl, 115 ex

FIELD: chemistry.

SUBSTANCE: invention relates to compounds of formula (I) or pharmaceutically acceptable salts, solvates or tautomers thereof, where substitute M is selected from groups D1 and D2, having structural formulae given below, and R1, E, A and X are as described in the formula of invention. Disclosed also are pharmaceutical compositions which contain these compounds, methods for synthesis of these compounds, intermediate compounds and synthesis methods thereof, as well as use of compounds of formula (I) in preventing or treating diseases mediated by CDK kinases, GSK-3 kinases or Aurora kinases.

EFFECT: high effectiveness of the compounds.

40 cl, 8 dwg, 18 tbl, 84 ex

Aromatic compound // 2416608

FIELD: chemistry.

SUBSTANCE: invention describes a novel compound of general formula (1), where radicals R1, R2, X1, Y and A are as described in claim 1 of the invention. The invention also describes a method of obtaining compounds of formula (1), as well as a pharmaceutical composition based on said compounds, for treating fibrosis.

EFFECT: novel compounds with excellent collagen formation suppression, cause fewer side-effects and which are safer are obtained.

62 cl, 2717 ex, 432 tbl

FIELD: chemistry.

SUBSTANCE: invention relates to novel benzo[d]isoxazol-3-ylamine compounds of formula I in free form or in form of salts with physiologically compatible acids, having antagonistic effect on KCNQ2/3 ion channel. In formula I , R1, R2, R3 and R4 independently denote H, F, CI, Br, I, -NR7R8, -OR9 or C1-C10alkyl, R5 denotes -C(=S)NR21R22 or (CHR6)n-R25, where n equals 1, 2 or 3, R6 denotes H or C1-C6 alkyl, R25 denotes aryl or heteroaryl, R7 and R8 independently denote H or C1-C10 alkyl, R9 denotes H, C1-C10alkyl or -(C1-C5alkylene)aryl, R21 denotes H, R22 denotes C1-C10alkyl, C2-C10alkenyl, C3-C8cycloalkyl, -(C1-C5alkylene)-C3-C8cycloalkyl, -(C1-C3alkylene)heterocycloalkyl, aryl, heteroaryl or -(C1-C5alkylene)aryl, wherein each of the heterocycloalkyl residues has 5-6 members, contains 1 or 2 heteroatoms in the ring, independently selected from oxygen and nitrogen, each of the aryl residues is phenyl, anthracenyl or naphthyl, each of the heteroaryl residues has 5 or 6 members and contains 1 or 2 heteroatoms in the ring, independently selected from oxygen, sulphur and nitrogen.

EFFECT: said compounds can be used to prepare a medicinal agent for curing pain, migraine, anxiety, uroclepsia or epilepsy.

17 cl, 203 ex

FIELD: chemistry.

SUBSTANCE: invention relates to compounds of formula 1, compounds of formula 5 and pharmaceutically acceptable salts thereof. In formulae 1 5 Y denotes -C(O)-, X denotes -N(R11)-, R1 denotes a residue of formula 1a or 1b - for formula 1 or residue of formulae 5a or 5b - for formula 5 1a 1b 5a 5b, R2 and R7 independently denote H, hydroxyl or (C1-C6)alkyl; R3 and R6 each independently denotes H, hydroxyl or (C1-C6)alkyl; R4 and R5 each independently denotes H or (C1-C6)alkyl; the rest of the radicals are described in the formula of invention. The invention also relates to separate compounds given in the formula of invention, a pharmaceutical composition having Bcl bound protein inhibiting properties, which contains a therapeutically effective amount of the disclosed compound, a method of treating a bc1 mediated disorder, involving introduction of a therapeutically effective amount of the disclosed compound and a method of treating a bc1 mediated disorder involving administration to a patient in need of treatment of an effective amount of camptothecin and therapeutically effective amount of the disclosed compound.

EFFECT: high efficiency of the composition.

84 cl, 12 tbl, 1 dwg, 217 ex

FIELD: chemistry.

SUBSTANCE: invention relates to a heterocyclic compound or salt thereof, having formula (1): where R2 is hydrogen or a lower alkyl group; A is a lower alkylene group or a lower alkenylene group and R1 is a cyclo(C3-C8)alkyl group, an aromatic group or a heterocyclic group selected from a group consisting of groups (I)-(IV), defined in the formula of invention. The invention also relates to a pharmaceutical composition, having activity as a partial agonist of dopamine D2 receptors and/or a serotonin 5-HT2A receptor antagonist and/or an adrenalin α1 receptor antagonist and/or a serotonin absorption inhibitor and/or serotonin reuptake inhibitor based on said compounds, a method of preparing a pharmaceutical composition, use of said compounds as a partial agonist of dopamine D2 receptors and/or a serotonin 5-HT2A receptor antagonist and/or an adrenalin α1 receptor antagonist and/or a serotonin absorption inhibitor and/or serotonin reuptake inhibitor, as well as a method of producing formula I compounds.

EFFECT: novel compounds are obtained and described, which have a wide range of curative effect on mental disorders, including central nervous system disorders, without side effects and with high degree of safety.

22 cl, 3110 ex, 314 tbl

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to new cyclopenta[b]benzofuranyl derivatives of formula wherein substitutes R1, R2, R3, R4, R5, R6 and R7 and n are specified in the patent clam. These compounds exhibit properties of NF-kB-activity and/or AP-1 inhibitor/modulator. Also, the inventive subject matter are methods for preparing intermediate compounds thereof, a pharmaceutical composition containing them, administration thereof for prevention and/or treatment of inflammatory and autoimmune diseases, neurodegenerative diseases and hyperproliferative diseases caused by NF-kB- and/or AP-1-activity, and a method for prevention and/or treatment of said diseases.

EFFECT: preparation of new cyclopenta[b]benzofuranyl derivatives.

21 cl, 3 tbl, 151 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: there are described 3,4-substituted piperidines applicable in diagnostics and drug therapy of a warm-blooded animal, preferentially for therapy of a disease which depends on renin activity; application of a compound of such kind for preparing a pharmaceutical composition for therapy of the disease which depends on renin activity; application of the compound of such kind for therapy of the disease which depends on renin activity; the pharmaceutical compositions containing 3,4-substituted piperidine, and/or a therapeutic mode involving administration of 3,4-substituted piperidine, a method for producing 3,4-substituted piperidine. The preferential compound (which also can be presented in the form of salts) are described by formula I' wherein R1, R2, T, R3 and R4 are such as described by the patent claim.

EFFECT: production of the compounds for therapy of the disease which depends on renin activity.

28 cl, 1 tbl, 375 ex

FIELD: chemistry.

SUBSTANCE: invention relates to azole derivatives of formula I , where: A denotes S, O; W denotes -(C=O)-; X are identical or different and denote =C(-R)- or =N-; Y denotes -O- or -NR1-; R denotes hydrogen, halogen, (C1-C6)-alkyl, nitro; R1 denotes hydrogen; R2 denotes (C5-C16)-alkyl, (C1-C4)alkyl-phenyl, where phenyl can be optionally mono- or poly-substituted with (C1-C6)-alkyl; R3 denotes hydrogen; or R2 and R3 together with the nitrogen atom bearing them can form a monocyclic saturated 6-member ring system, where separate members of this ring system can be substituted with 1 group selected from the following: -CHR5-, -NR5-; R5 denotes (C1-C6)-alkyl, trifluoromethyl; and physiologically acceptable salts thereof. The invention also pertains to methods of producing said compounds and a medicinal agent based on said compounds.

EFFECT: novel compounds and a medicinal agent based on said compounds are obtained, which can be used as hormone-sensitive lipase (HSL) or endothelial lipase (EL) inhibitors.

12 cl, 11 ex

FIELD: chemistry.

SUBSTANCE: invention relates to a heterocyclic compound or salt thereof, having formula (1): where R2 is hydrogen or a lower alkyl group; A is a lower alkylene group or a lower alkenylene group and R1 is a cyclo(C3-C8)alkyl group, an aromatic group or a heterocyclic group selected from a group consisting of groups (I)-(IV), defined in the formula of invention. The invention also relates to a pharmaceutical composition, having activity as a partial agonist of dopamine D2 receptors and/or a serotonin 5-HT2A receptor antagonist and/or an adrenalin α1 receptor antagonist and/or a serotonin absorption inhibitor and/or serotonin reuptake inhibitor based on said compounds, a method of preparing a pharmaceutical composition, use of said compounds as a partial agonist of dopamine D2 receptors and/or a serotonin 5-HT2A receptor antagonist and/or an adrenalin α1 receptor antagonist and/or a serotonin absorption inhibitor and/or serotonin reuptake inhibitor, as well as a method of producing formula I compounds.

EFFECT: novel compounds are obtained and described, which have a wide range of curative effect on mental disorders, including central nervous system disorders, without side effects and with high degree of safety.

22 cl, 3110 ex, 314 tbl

FIELD: medicine, pharmaceutics.

SUBSTANCE: claimed invention relates to novel substituted imidazole compounds of formula I where values of radicals are given in description, as well as to their based on them pharmaceutical compositions.

EFFECT: formula I compounds, as well as their salts, esters and compositions based on them possess ability to inhibit protein of kinesin spindle (KSP) and can be used for treatment of cancer diseases.

40 cl, 15 ex, 3 tbl

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention relates to novel compounds of formula: I, where R1 is selected from group, consisting of ethyl, 2-fluorethyl and isopropyl; R2 is selected from group, consisting of hydrogen, C1-7-alkyl, hydroxy, C1-7-alkoxy, C3-7-cycloalkyl, halogen, -C(O)OR6, where R6 represents C1-7-alkyl, amino, phenyl, phenyl, substituted with 1-3 substituents, selected from group, consisting of halogen, halogen-C1-7-alkyl and halogen-C1-7-alkoxy, pyridyl, imidazolyl, triazolyl and pyrrolyl; R3 is selected from group, consisting of hydrogen, C1-7-alkoxy, amino, -O-benzyl and -o-tetrahydropyranyl; or R2 and R3 are bound to each other with formation of cycle together with carbon atoms to which they are bound, and R2 and R3 together represent -CH=CH-NH-; R4 is selected from group, consisting of hydrogen, halogen, pyridyl and pyrimidyl; R5 and R5' independently on each other are selected from hydrogen or methyl; A is selected from group, consisting of isphenyl; phenyl, substituted with 1-3 substituents, selected from group, consisting of C1-7-alkyl, C3-7-cycloalkyl, C1-7-alkylsulfonyl, -O-C1-7-alkylsulfonyl, hydroxy, C1-7-alkoxy, hydroxy-C1-7-alkyl, hydroxy-C2-7-alkoxy, dihydroxy-C3-7-alkoxy, C1-7-alkylamino, di-C1-7-alkylamino, amino-C2-7-alkoxy, amino-C1-7-alkyl, -C(O)NR10R11, -O-C1-7-alkylene-C(O)NR10R11, -C(O)OR10, -C1-7-alkylene-C(O)OR10, -O-C1-7-alkylene-C(O)OR10, halogen, halogen-C1-7-alkoxy, cyano- C1-7-alkoxy, fluorphenyl, pyridyl, tetrazolyl and tetrazolyl- C1-7-alkoxy; 1,3-benzodioxolyl; naphtyl; pyrimidinyl; pyridyl, substituted with one or two substituents, selected from group, consisting of C1-7-alkyl, C1-7-alkoxy, amino, C1-7-alkylamino, di-C1-7-alkylamino, C3-7-cycloalkylamino, halogen, cyano, morpholinyl, imidazolyl and -NH-C(O)-R9, where R9 represents C1-7-alkyl or C3-7-cycloalkyl, and indolyl; R10 and R11 independently on each other represent hydrogen or C1-7-alkyl; and to their pharmaceutically accdeptable salts. Invention also relates to pharmaceutical compositions.

EFFECT: obtaining novel biologically active compounds, which are antagonists of somatostatin receptor subtype 5 (SSTR5).

26 cl, 266 ex

FIELD: chemistry.

SUBSTANCE: invention describes a compound of formula I or its pharmaceutically acceptable salt , where R, R9, Z, X, Q and Y are defined in the formula of invention. The compounds are chemokine receptor 2 and chemokine receptor 5 antagonists and can be used as a medicinal agent for preventing, relieving or treating autoimmune or inflammatory diseases or conditions.

EFFECT: obtaining a formula (I) compound, a pharmaceutical composition based on the formula (I) compound, use of the compound in paragraph 1 to prepare a medicinal agent for treating an autoimmune or inflammatory disease or condition, as well as use of the compound in paragraph 1 to prepare a medicinal agent for treating HIV infection or AIDS.

11 cl, 181 ex

FIELD: chemistry.

SUBSTANCE: invention refers to novel method of obtaining [2S*[R*[R*[R*]]]] and [2R*[S*[S*[S*]]]]-(±)α,α'-[iminobis(methylene)]bis[6-fluoro-3,4-dihydro-2H-1-benzopyrane-2-methanol] racemate of the formula (I) (nebivolol) and its pharmaceutically acceptable salts , involving stages indicated in the claim, and to intermediate compounds and methods of obtainment thereof.

EFFECT: improved method.

106 cl, 12 tbl, 20 ex

FIELD: chemistry.

SUBSTANCE: invention relates to an improved method of producing 2H-1-benzopyran-2-methanol-α,α'-[iminobis(methylene)]bis[6-fluoro-3,4-dihydro-[2R*[R*[R*(S*)]]]], i.e. a nebivolol base of formula (IX), or its hydrochloride salt

as well as to a method of producing an intermediate compound - benzylated nebivolol of formula (VIII),

EFFECT: invention also relates to a pharmaceutical composition with antihypertensive action without using a wetting agent, and to a tablet containing this pharmaceutical composition.

21 cl, 20 tbl, 21 ex

FIELD: medicine.

SUBSTANCE: invention relates to 2,4-pyrimidindiamins, such as N4-(4-Chlorine-3-methoxyphenyl)-5-fluorine-N2-[3-(N-ethylamino)carbonylmethylenoxyphenyl]-2,4-pyrimidindiamin, N4-(3-Chlorine-4-methjopxycarbonylmethylenoxyphenyl)-5-fluorine- N2-[3-(N-methylamino)carbonylmethylenoxyphenyl]-2,4-pyrimidindiamin, N4-[3-Chlorine-4-(N-methylamino)carbonylmethylenoxyphenyl]-5-fluorine-N2-[3-(]N methylamino)carbonylmethylenoxyphenyl]- 2,4-pyrimidindiamin, N4-[3-Chlorine-4-(2-hydroxyethylenoxy)phenyl]-5-fluorine-N2-[3-(N- methylamino)carbonylmethylenoxyphenyl]- 2,4-pyrimidindiamin and other compounds given in item 1 of claimed invention as Syk-kinase inhibitors, as well as to based on them pharmaceutical composition and their application.

EFFECT: claimed compounds can be applied for treatment of autoimmune diseases, systemic http://lingvo.yandex.ru/?text=lupus%20erythematosus, rheumatoid arthritis, etc.

12 cl, 27 dwg, 11 tbl, 1797 ex

FIELD: chemistry.

SUBSTANCE: invention refers to new compounds of general formula (I) where R1 stands for hydrogen or linear, branched, saturated or unsaturated hydrocarbon radical; D stands for nitrogen atom or C-R2; E stands for nitrogen atom or C-R3; F stands for nitrogen atom or C-R4; G stands for nitrogen atom or C-R5; R2, R3, R4 and R5 are identical or different and individually represent hydrogen, halogen, alkoxy, linear or branched, saturated or unsaturated hydrocarbon radical; W stands for oxygen atom; X stands for radical of formula radical -(CH2)k-C(O)-(CH2)m-, -(CH2)n- or -(CH2)r-O-(CH2)s-, where k, m, r and s are equal to integers 0 to 6, and n is equal to an integer 1 to 6. Said radicals are optionally substituted with one or more substitutes independently chosen from the group consisting of R7; Y stands for radical of formula radical -(CH2)i-NH-C(O)-(CH2)j-, -(CH2)n-, -(CH2)r-O-(CH2)s-, -(CH2)t-NH-(CH2)u-, where i, j, n, r, s, t and u are equal to integers 0 to 6. Said radicals are optionally substituted C1-3alkyl, or C1-3alkyl-C1-3alkylsulphonylamino; radicals R7, B, R8, A, R9 are as it is presented in the patent claim. The invention also describes the pharmaceutical composition possessing inhibitory activity of receptor tyrosine kinase to KDR receptor including described compounds.

EFFECT: compounds possess inhibitory activity of receptor tyrosine kinase to KDR receptor and can be effective in therapy of the diseases associated uncontrolled angiogenesis.

29 cl, 746 ex, 6 tbl

FIELD: chemistry, pharmacology.

SUBSTANCE: present invention relates to new compounds with formula (I), their esters, carbamates and pharmaceutically used salts, which can be used as inhibitors of p38 kinase, which means they can be used for curing diseases and conditions for which p38 is the mediator. In formula (I): Q represents -C(R1R2R3); R1 is chosen from hydrogen, C1-C8 alkyl, hydroxyC1-C8alkyl, and C1-C8alkoxy C1-C8alkyl; R2 and R3 are chosen: (i) independently from: (a) hydrogen, under the condition that, if R1 represents hydrogen, then only one of R2 and R3 can be chosen from hydrogen; (b) C1-C8alkyl; C1-C8alkyl, substituted with one or two radicals halogen, -OR8, -S(O)pR10;(c) -OR8; or (ii) R2 and R3 together with the carbon atom to which they are bonded, form optionally substituted C3-C7cycloalkyl or substituted heterocyclic ring system; R4 and R5 are independently chosen from halogen; R8 and R9 are independently chosen from hydrogen, C1-C8alkyl; R10 represents C1-C8alkyl; m equals 0, n equals 0; and p equals 2; where the term "substituted cycloalkyl" stands for a cycloalkyl group, containing one or two substitutes, which are independently chosen from a group, consisting of -Y-ORs, -Y-S(O)0-2RS, C(=O)ORs, where Y is absent; Rs is independently chosen from hydrogen, C1-C8alkyl, except when the said substitute represents -Y-S(O)1-2Rs, then RS represents hydrogen; the term "heterocyclic ring system" stands for a saturated non-aromatic monocyclic fragment, consisting of 5 to 6 atoms, which are part of the ring system, from which one atom, which is part of the ring system, is a heteroatom, chosen from N, O, and the rest of the atoms in the ring system are carbon atoms; the term "substituted heterocyclic ring system" stands for a heterocyclic fragment mentioned above, containing one substitute, chosen from the group, -Y-Rs, -Y-ORs, -Y-C(O)2Rs, -Y-S(O)0-2Rs, where Y is absent or represents a C1-C4alkylene group, Rs represents the same as was defined above for the substituted cycloalkyl group.

EFFECT: used for treating diseases and conditions.

13 cl, 2 dwg, 5 tbl, 17 ex

FIELD: chemistry.

SUBSTANCE: invention concerns novel amidomethyl-substituted derivatives of 2-(4-sulfonylamino)-3-hydroxy3,4-dihydro-2N-chromen-6-yl of the general formula (I) where R1 is C1-C4alkyl, R2 is C1-C4alkyl, R3 is phenyl optionally once or twice substituted or substituted by halogen, C1-C4alkyl, C1-C4alkoxy group or trifluoromethyl, naphthyl or biphenyl, R4 is hydrogen, C1-C6alkyl or C3-C7cycloalkyl-C1-C4alkyl, R5 is hydrogen, and R6 is C1-C6 alkyl, phenyl-C1-C4alkyl, phenyl group optionally substituted by halogen, furyl-C1-C4alkyl or tetrahydronaphthyl, or R5 and R6 together with nitrogen atom linking them form piperazine ring optionally substituted by phenyl.

EFFECT: also invention claims method of obtaining claimed compounds, and intermediary products used in method implementation, as well as medicines containing compounds of the formula (I) with antiarrhythmic effect, and application of these medicines.

11 cl, 6 tbl, 6 ex

FIELD: chemistry.

SUBSTANCE: present invention relates to hot or sweet flavourants in form of a synthetic amide compound or edible salt thereof in amount ranging from approximately 0.001 parts per million to approximately 100 parts per million. The amide compound has formula

where A is a phenyl or a 5- or 6-member heteroaryl ring selected from a group comprising pyridine, pyrazine, pyrazole, thiazole, furan, thiophene, benzofuran and benzothiophene; m equals 1, 2 or 3, each R1 is independently selected from hydroxyl, fluorine, chlorine, SEt, SCH3, methyl, ethyl, isopropyl, vinyl, trifluoromethyl, methoxy, ethoxy and isopropoxy, or alternatively two R1 are bonded to form a saturated C1-C3 alkylenedioxy ring on the phenyl; and R2 is a C3-C10 branched alkyl. The amide compound also has formula

in which substitutes A, B, R50, R60, R70, R80, n and m assume values given in the formula of invention. The amide compound is also a specific chemical compound.

EFFECT: obtaining hot and sweet taste modifiers and boosters for food and medicinal products.

39 cl, 7 tbl, 180 ex

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