New 2-aminooxazolines as taar1 ligands for cns diseases

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to the use of compounds of formula (wherein R1, R2, X, Y and n have the values specified in the patent claim) or their pharmaceutically acceptable salts for treating the diseases related to the biological function of the trace amine associated receptors, namely depression, anxiety disorders, bipolar disorders, attention deficit/hyperactivity disorder, stress-induced disorders, schizophrenia, neurological disorders, Parkinson's disease, neurodegenerative disorders, Alzheimer's disease, epilepsy, migraine, addictions, metabolic disorders, eating disorders, diabetes, diabetic complications, obesity, dyslipidemia, energy consumption and assimilation disorders, thermal homeostasis disorders and disturbances, sleeping and circadian rhythm disorders, and cardiovascular diseases. Besides, the invention refers to compounds of formulas I-A, I-B, I-C, I-D, l-E, l-F, I-G, I-H (structural formulas of which are presented in the patent claim) and to a pharmaceutical composition based on the compounds of formula (I) for treating the diseases related to the biological function of the trace amine associated receptors.

EFFECT: use of the compounds of formula 1 in preparing the drugs for treating the diseases related to the biological function of the trace amine associated receptors.

45 cl, 9 dwg, 1 tbl, 379 ex

 

The text descriptions are given in facsimile form.

1. The use of the compounds of formula

where R1represents a hydrogen atom, a tritium, With1-7alkyl, C1-7alkoxy, C1-7alkyl, substituted by a halogen atom, a C1-7-alkoxy substituted by halogen atom, halogen atom, phenyl, possibly substituted by a halogen atom, or represents phenyloxy, benzyloxy, -COO-C1-7alkyl, -O-(CH2)o-O-C1-7-alkyl, NH-C3-6-cycloalkyl,3-6-cycloalkyl or tetrahydropyran-4-yloxy, where n>1 these substituents may be the same or different;
X represents a bond, -CHR-, -CHRCHR'-, -och2-, -CH2OCHR-, -CH2CH2CH2, -SCH2-, -S(O)2CH2-, -CH2SCH2-, -CH2N(R)CH2-, -C3-6cycloalkyl-CH 2or SiRR'-CH2-except that when X represents-och2-group C1-7-alkoxy (R1) is not in the 2nd position on Y;
R/R' independently of one another can represent a hydrogen atom, a C1-7-alkyl or C1-7-alkyl, substituted by a halogen atom;
R2represents a hydrogen atom or a C1-7-alkyl;
Y represents phenyl, naphthyl, thiophenyl, pyridinyl,3-6-cycloalkyl, 1,2,3,4-tetrahydro-naphthalene-2-yl, 2,3-dihydrobenzo[1,4]dioxin-6-yl or benzo[1,3]dioxol-5-yl;
n is 0, 1, 2 or 3;
o has a value of 2 or 3;
or a pharmaceutically acceptable salt accession acid in the manufacture of medicaments for the treatment of diseases associated with the biological function of the receptor associated with the trace amines (trace amine associated receptors), namely, anxiety disorders, bipolar disorder, attention deficit disorder and hyperactivity disorder, disorders caused by stress, psychotic disorders, schizophrenia, neurological diseases, Parkinson's disease, neurodegenerative disorders, Alzheimer's disease, epilepsy or migraine.

2. The use of the compounds of formula I according to claim 1, where X represents the connection.

3. The use of the compounds of formula I according to claim 2, where Y is phenyl, substituted by one or more than one atom ha is Ohana.

4. The use of the compounds of formula I according to claim 3, where these compounds are
(S)-4-(2-chloro-phenyl)-4,5-dihydro-oxazol-2-ylamine,
(RS)-4-(4-chloro-phenyl)-4,5-dihydro-oxazol-2-ylamine,
(RS)-4-(2,4-debtor-phenyl)-4,5-dihydro-oxazol-2-ylamine,
(S)-4-(2,3-debtor-phenyl)-4,5-dihydro-oxazol-2-ylamine,
(RS)-4-(3,4-dichlorophenyl)-4,5-dihydro-oxazol-2-ylamine,
(RS-4-(2,5-debtor-phenyl)-4,5-dihydro-oxazol-2-ylamine,
(RS)-4-(2,3,4-Cryptor-phenyl)-4,5-dihydro-oxazol-2-ylamine,
(RS)-4-(3-chloro-2-fluoro-phenyl)-4,5-dihydro-oxazol-2-ylamine,
(RS)-4-(5-chloro-2-fluoro-phenyl)-4,5-dihydro-oxazol-2-ylamine,
(RS)-4-(4-bromo-phenyl)-4,5-dihydro-oxazol-2-ylamine,
(S)-4-(3-bromo-2,4-debtor-phenyl)-4,5-dihydro-oxazol-2-ylamine,
(S)-4-(2,4-debtor-phenyl)-4,5-dihydro-oxazol-2-ylamine,
(S)-4-(3,4-dichloro-phenyl)-4,5-dihydro-oxazol-2-ylamine,
(S)-4-(2,5-debtor-phenyl)-4,5-dihydro-oxazol-2-ylamine,
(S)-4-(4-bromo-phenyl)-4,5-dihydro-oxazol-2-ylamine,
(S)-4-(2,4,5-Cryptor-phenyl)-4,5-dihydro-oxazol-2-ylamine,
(S)-4-(3-chloro-2-fluoro-phenyl)-4,5-dihydro-oxazol-2-ylamine,
(S)-4-(2,3,5-Cryptor-phenyl)-4,5-dihydro-oxazol-2-ylamine,
(S)-4-(3,4-dichloro-phenyl)-4-methyl-4,5-dihydro-oxazol-2-ylamine,
(S)-4-(4-chloro-phenyl)-4-methyl-4,5-dihydro-oxazol-2-ylamine,
(S)-4-(3,4-debtor-phenyl)-4,5-dihydro-oxazol-2-ylamine,
(S)-4-(2,3-dichloro-phenyl)-4,5-dihydro-oxazol-2-ylamine,
(S)-4-(4-chloro-phenyl)-4,5-dihydro-oxazol-2-ylamine,
(S)-4-(3,4,5-Cryptor-phenyl)-4,5-dihydro-oxazol-2-ylamine,
(S)-4-(3-the ers-4-fluoro-phenyl)-4,5-dihydro-oxazol-2-ylamine,
(S)-4-(4-chloro-3-fluoro-phenyl)-4,5-dihydro-oxazol-2-ylamine,
(S)-4-(3,5-debtor-phenyl)-4,5-dihydro-oxazol-2-ylamine,
(S)-4-(3-chloro-5-fluoro-phenyl)-4,5-dihydro-oxazol-2-ylamine,
(S)-4-(2-chloro-phenyl)-4-methyl-4,5-dihydro-oxazol-2-ylamine,
(RS)-4-(3-chloro-phenyl)-4,5-dihydro-oxazol-2-ylamine,
(RS)-4-(3-bromo-phenyl)-4,5-dihydro-oxazol-2-ylamine,
(S)-4-(2,5-debtor-phenyl)-4-methyl-4,5-dihydro-oxazol-2-ylamine,
(RS)-4-(3-fluoro-phenyl)-4,5-dihydro-oxazol-2-ylamine,
(RS)-4-(3,5-dichloro-phenyl)-4,5-dihydro-oxazol-2-ylamine,
(+)-(S)-4-(5-chloro-2-fluoro-phenyl)-4,5-dihydro-oxazol-2-ylamine,
(+)-(S)-4-(3-chloro-phenyl)-4,5-dihydro-oxazol-2-ylamine,
(S)-4-(2-fluoro-phenyl)-4-methyl-4,5-dihydro-oxazol-2-ylamine,
(+)-(S)-4-(3-bromo-phenyl)-4,5-dihydro-oxazol-2-ylamine,
(+)-(S)-4-(3-fluoro-phenyl)-4,5-dihydro-oxazol-2-ylamine,
(+)-(S)-4-(3,5-dichloro-phenyl)-4,5-dihydro-oxazol-2-ylamine,
(S)-4-(2,4-debtor-phenyl)-4-methyl-4,5-dihydro-oxazol-2-ylamine,
(RS)-4-methyl-4-(2,3,5-Cryptor-phenyl)-4,5-dihydro-oxazol-2-ylamine,
(S)-4-(4-bromo-phenyl)-4-methyl-4,5-dihydro-oxazol-2-ylamine,
(RS)-4-(2,4-dichloro-phenyl)-4,5-dihydro-oxazol-2-ylamine,
(S)-4-(4-chloro-3-fluoro-phenyl)-4-methyl-4,5-dihydro-oxazol-2-ylamine,
(RS)-4-(2-bromo-phenyl)-4,5-dihydro-oxazol-2-ylamine,
(RS)-4-methyl-4-(2,4,5-Cryptor-phenyl)-4,5-dihydro-oxazol-2-ylamine,
(RS)-4-(4-bromo-3-fluoro-phenyl)-4,5-dihydro-oxazol-2-ylamine,
(RS)-4-(2,5-dichloro-phenyl)-4,5-dihydro-oxazol-2-ylamine,
(+)-(S)-4-(2-bromo-phenyl)-4,5-dihydro-oxazol-2-ylamine,
(S)-4-(3-chloro-ftor-phenyl)-4-methyl-4,5-dihydro-oxazol-2-ylamine,
(RS)-4-methyl-4-(2,3,4-Cryptor-phenyl)-4,5-dihydro-oxazol-2-ylamine,
(S)-4-(5-chloro-2-fluoro-phenyl)-4-methyl-4,5-dihydro-oxazol-2-ylamine,
(RS)-4-methyl-4-(4-chloro-2,5-debtor-phenyl)-4,5-dihydro-oxazol-2-ylamine,
(RS)-4-methyl-4-(3,4,5-Cryptor-phenyl)-4,5-dihydro-oxazol-2-ylamine,
(S)-4-(3-chloro-4-fluoro-phenyl)-4-methyl-4,5-dihydro-oxazol-2-ylamine,
(S)-4-(4-chloro-2,5-debtor-phenyl)-4-methyl-4,5-dihydro-oxazol-2-ylamine,
(RS)-4-(4-bromo-2-chloro-phenyl)-4,5-dihydro-oxazol-2-ylamine,
(RS)-4-(2,4-dichloro-phenyl)-4-methyl-4,5-dihydro-oxazol-2-ylamine,
(-)-(R)-4-(2,4-dichloro-phenyl)-4,5-dihydro-oxazol-2-ylamine,
(+)-(S)-4-(2,4-dichloro-phenyl)-4,5-dihydro-oxazol-2-ylamine,
(+)-(S)-4-(2,5-dichloro-phenyl)-4,5-dihydro-oxazol-2-ylamine,
(RS)-4-(2,5-dichloro-phenyl)-4-methyl-4,5-dihydro-oxazol-2-ylamine,
(+)-(S)-4-(2,3,4-Cryptor-phenyl)-4,5-dihydro-oxazol-2-ylamine,
(S)-4-methyl-4-(3,4,5-Cryptor-phenyl)-4,5-dihydro-oxazol-2-ylamine,
(RS)-4-(3-(chloro-2-fluoro-phenyl)-4-methyl-4,5-dihydro-oxazol-2-ylamine,
(S)-4-(4-chloro-phenyl)-4-ethyl-4,5-dihydro-oxazol-2-ylamine,
(-)-(R)-4-(4-bromo-2-chloro-phenyl)-4,5-dihydro-oxazol-2-ylamine,
(+)-(S)-4-(4-bromo-2-chloro-phenyl)-4,5-dihydro-oxazol-2-ylamine,
(RS)-4-(2-chloro-4-fluoro-phenyl)-4-methyl-4,5-dihydro-oxazol-2-ylamine,
(+)-(S)-4-(4-bromo-3-fluoro-phenyl)-4,5-dihydro-oxazol-2-ylamine,
(RS)-4-(4-bromo-3-chloro-phenyl)-4,5-dihydro-oxazol-2-ylamine,
(S)-4-(3,4-dichloro-phenyl)-4-ethyl-4,5-dihydro-oxazol-2-ylamine,
(+)-(8)-4-(4-bromo-3-chloro-phenyl)-4,5-dihydro-oxazol-2-ylamine,
(RS)-4-(4-bro is-2-fluoro-phenyl)-4,5-dihydro-oxazol-2-ylamine or
(S)-4-(4-bromo-2-fluoro-phenyl)-4,5-dihydro-oxazol-2-ylamine.

5. The use of the compounds of formula 1 according to claim 2, where Y represents phenyl, substituted CH3, CF3The co3, OCF3or och2-phenyl.

6. The use of the compounds of formula 1 according to claim 5, which is a
(RS)-4-(2-trifluoromethyl-phenyl)-4,5-dihydro-oxazol-2-ylamine,
(RS)-4-ortho-tolyl-4,5-dihydro-oxazol-2-ylamine,
(RS)-4-(4-triptoreline-phenyl)-4,5-dihydro-oxazol-2-ylamine,
(RS)-4-(4-methoxy-3-methyl-phenyl)-4,5-dihydro-oxazol-2-ylamine,
(S)-4-ortho-tolyl-4,5-dihydro-oxazol-2-ylamine,
(RS)-4-(4-benzyloxy-phenyl)-4,5-dihydro-oxazol-2-ylamine,
(S)-4-(2-trifluoromethyl-phenyl)-4,5-dihydro-oxazol-2-ylamine,
(S)-4-(4-methoxy-3-methyl-phenyl)-4,5-dihydro-oxazol-2-ylamine,
(S)-4-methyl-4-(4-trifluoromethyl-phenyl)-4,5-dihydro-oxazol-2-ylamine,
(S)-4-(3-trifluoromethyl-phenyl)-4,5-dihydro-oxazol-2-ylamine,
(S)-4-methyl-4-para-tolyl-4,5-dihydro-oxazol-2-ylamine,
(S)-4-methyl-4-(3-trifluoromethyl-phenyl)-4,5-dihydro-oxazol-2-ylamine,
(RS)-4-(4-methoxy-2-trifluoromethyl-phenyl)-4,5-dihydro-oxazol-2-ylamine,
(+)-(S)-4-(4-methoxy-2-trifluoromethyl-phenyl)-4,5-dihydro-oxazol-2-ylamine.

7. The use of the compounds of formula 1 according to claim 2, where Y represents phenyl substituted by phenyl, which may have as a substituent a halogen atom.

8. The use of the compounds of formula 1 according to claim 7, which is a
(RS)-4-biphenyl-4-and the -4,5-dihydro-oxazol-2-ylamine,
(S)-4-biphenyl-4-yl-4,5-dihydro-oxazol-2-ylamine or
(RS)-4-(4'-chloro-biphenyl-4-yl)-4,5-dihydro-oxazol-2-ylamine.

9. The use of the compounds of formula 1 according to claim 2, where Y represents phenyl, substituted och3or a halogen atom and CF3, a halogen atom and CH3, a halogen atom and C3-6-cycloalkyl or a halogen atom and co3.

10. The use of the compounds of formula I according to claim 9, where these compounds are
(RS)-4-(3-chloro-4-methoxyphenyl)-4,5-dihydro-oxazol-2-ylamine,
(S)-4-(3-chloro-4-methoxy-phenyl)-4,5-dihydro-oxazol-2-ylamine,
(S)-4-(2-fluoro-4-trifluoromethyl-phenyl)-4-methyl-4,5-dihydro-oxazol-2-ylamine,
(RS)-4-(4-fluoro-2-trifluoromethyl-phenyl)-4,5-dihydro-oxazol-2-ylamine,
(RS)-4-(5-chloro-2-trifluoromethyl-phenyl)-4,5-dihydro-oxazol-2-ylamine,
(RS)-4-(4-chloro-2-trifluoromethyl-phenyl)-4,5-dihydro-oxazol-2-ylamine,
(RS)-4-(4,5-dichloro-2-trifluoromethyl-phenyl)-4,5-dihydro-oxazol-2-ylamine,
(+)-(S)-4-(4-chloro-2-trifluoromethyl-phenyl)-4,5-dihydro-oxazol-2-ylamine,
(+)-(S)-4-(4,5-dichloro-2-trifluoromethyl-phenyl)-4,5-dihydro-oxazol-2-ylamine,
(-)-(S)-4-(4,5-dichloro-2-trifluoromethyl-phenyl)-4,5-dihydro-oxazol-2-ylamine,
(+)-(S)-4-(4-fluoro-2-trifluoromethyl-phenyl)-4,5-dihydro-oxazol-2-ylamine,
(RS)-4-(5-fluoro-2-trifluoromethyl-phenyl)-4,5-dihydro-oxazol-2-ylamine,
(RS)-4-(5-fluoro-2-methyl-phenyl)-4,5-dihydro-oxazol-2-ylamine,
(+)-(S)-4-(5-fluoro-2-trifluoromethyl-phenyl)-4,5-dihydro-oxazol-2-ylamine,
(RS)-4-(4-chloro-3-IU the Il-phenyl)-4-methyl-4,5-dihydro-oxazol-2-ylamine,
(RS)-4-(5-chloro-2-methyl-phenyl)-4,5-dihydro-oxazol-2-ylamine,
(RS)-4-(4-chloro-2-fluoro-5-methyl-phenyl)-4-methyl-4,5-dihydro-oxazol-2-ylamine,
(S)-4-(4-chloro-3-methyl-phenyl)-4-methyl-4,5-dihydro-oxazol-2-ylamine,
(RS)-4-(4-bromo-2-trifluoromethyl-phenyl)-4,5-dihydro-oxazol-2-ylamine,
(S)-4-(4-chloro-2-fluoro-5-methyl-phenyl)-4-methyl-4,5-dihydro-oxazol-2-ylamine,
(+)-(S)-4-(5-chloro-2-methyl-phenyl)-4,5-dihydro-oxazol-2-ylamine,
(RS)-4-(4-fluoro-2-methyl-phenyl)-4,5-dihydro-oxazol-2-ylamine,
(+)-(S)-4-(4-bromo-2-trifluoromethyl-phenyl)-4,5-dihydro-oxazol-2-ylamine,
(+)-(S)-4-(5-chloro-2-trifluoromethyl-phenyl)-4,5-dihydro-oxazol-2-ylamine,
(RS)-4-(4-chloro-2-ethyl-phenyl)-4,5-dihydro-oxazol-2-ylamine,
(+)-(S)-4-(4-fluoro-2-methyl-phenyl)-4,5-dihydro-oxazol-2-ylamine,
(RS)-4-(3-chloro-4-methyl-phenyl)-4,5-dihydro-oxazol-2-ylamine,
(RS)-4-(4-chloro-2-cyclopropyl-phenyl)-4,5-dihydro-oxazol-2-ylamine,
(S)-4-(4-chloro-2-ethyl-phenyl)-4,5-dihydro-oxazol-2-ylamine,
(RS)-4-(3-fluoro-2-methyl-phenyl)-4,5-dihydro-oxazol-2-ylamine,
(S)-4-(4-chloro-2-cyclopropyl-phenyl)-4,5-dihydro-oxazol-2-ylamine,
(RS)-4-(3-fluoro-2-trifluoromethyl-phenyl)-4,5-dihydro-oxazol-2-ylamine or
(S)-4-(3-chloro-4-methyl-phenyl)-4,5-dihydro-oxazol-2-ylamine.

11. The use of the compounds of formula I according to claim 1, where X represents the CHR and Y is phenyl.

12. The use of the compounds of formula I according to claim 11, which is a
(S)-4-(2-chloro-benzyl)-4,5-dihydro-oxazol-2-ylamine,
(S)-4-(3-trifluoromethyl-benzyl)-4,5-dihyd the o-oxazol-2-ylamine or
(RS)-4-(2-fluoro-5-methyl-benzyl)-4,5-dihydro-oxazol-2-ylamine.

13. The use of the compounds of formula I according to claim 1, where X represents CHRCHR' and Y is phenyl.

14. The use of the compounds of formula I according to item 13, which is a
(R)-4-phenethyl-4,5-dihydro-oxazol-2-ylamine,
(S)-4-phenethyl-4,5-dihydro-oxazol-2-ylamine,
(RS)-4-methyl-4-phenethyl-4,5-dihydro-oxazol-2-ylamine,
(S)-4-methyl-4-phenethyl-4,5-dihydro-oxazol-2-ylamine,
(RS)-4-phenethyl-4,5-dihydro-oxazol-2-ylamine,
(S)-4-[2-(4-fluoro-phenyl)-ethyl]-4,5-dihydro-oxazol-2-ylamine,
(S)-4-[2-(4-fluoro-3-methoxy-phenyl)-ethyl]-4,5-dihydro-oxazol-2-ylamine,
((S)-4-[2-(2,4-debtor-phenyl)-ethyl]-4,5-dihydro-oxazol-2-ylamine,
(S)-4-[2-(3,4-debtor-phenyl)-ethyl]-4,5-dihydro-oxazol-2-ylamine,
(S)-4-[2-(2-trifluoromethyl-phenyl)-ethyl]-4,5-dihydro-oxazol-2-ylamine,
(S)-4-[2-(2-fluoro-phenyl)-ethyl]-4,5-dihydro-oxazol-2-ylamine,
(S)-4-[2-(3-fluoro-phenyl)-ethyl]-4,5-dihydro-oxazol-2-ylamine,
(S)-4-[2-(3,5-debtor-phenyl)-ethyl]-4,5-dihydro-oxazol-2-ylamine,
(S)-4-(2-ortho-tolyl-ethyl)-4,5-dihydro-oxazol-2-ylamine,
(S)-4-(2-meta-tolyl-ethyl)-4,5-dihydro-oxazol-2-ylamine,
(S)-4-(2-para-tolyl-ethyl)-4,5-dihydro-oxazol-2-ylamine,
(S)-4-[2-(4-trifluoromethyl-phenyl)-ethyl]-4,5-dihydro-oxazol-2-ylamine,
(S)-4-[2-(3-trifluoromethyl-phenyl)-ethyl]-4,5-dihydro-oxazol-2-ylamine,
(R)-4-[2-(3,4-dichloro-phenyl)-ethyl]-4,5-dihydro-oxazol-2-ylamine,
(S)-4-[2-(3,4-dichloro-phenyl)-ethyl]-4,5-dihydro-oxazol-2-ylamine,
(S)-4-[2-(4-x is the PR-2-fluoro-phenyl)-ethyl]-4,5-dihydro-oxazol-2-ylamine,
(S)-4-[2-(4-fluoro-3-trifluoromethyl-phenyl)-ethyl]-4,5-dihydro-oxazol-2-ylamine,
(S)-4-[2-(3-fluoro-4-trifluoromethyl-phenyl)-ethyl]-4,5-dihydro-oxazol-2-ylamine,
(S)-4-[2-(3,5-dichloro-phenyl)-ethyl]-4,5-dihydro-oxazol-2-ylamine,
(S)-4-[2-(2-chloro-4-fluoro-phenyl)-ethyl]-4,5-dihydro-oxazol-2-ylamine,
(S)-4-[2-(4-fluoro-3-methyl-phenyl)-ethyl]-4,5-dihydro-oxazol-2-ylamine,
(S)-4-{2-[3-(1,1,2,2-titrator-ethoxy)-phenyl]-ethyl}-4,5-dihydro-oxazol-2-ylamine,
(S)-4-[2-(2-fluoro-3-trifluoromethyl-phenyl)-ethyl]-4,5-dihydro-oxazol-2-ylamine,
(S)-4-[2-(3-bromo-phenyl)-ethyl]-4,5-dihydro-oxazol-2-ylamine,
(S)-4-[2-(4-chloro-3-trifluoromethyl-phenyl)-ethyl]-4,5-dihydro-oxazol-2-ylamine,
(S)-4-[2-(3-fluoro-4-triptoreline-phenyl)-ethyl]-4,5-dihydro-oxazol-2-ylamine,
(S)-4-[2-(4-fluoro-3-triptoreline-phenyl)-ethyl]-4,5-dihydro-oxazol-2-ylamine,
(S)-4-[2-(2,3-dichloro-phenyl)-ethyl]-4,5-dihydro-oxazol-2-ylamine,
(S)-4-[2-(3-chloro-4-triptoreline-phenyl)-ethyl]-4,5-dihydro-oxazol-2-ylamine,
(S)-4-[2-(2-chloro-3-trifluoromethyl-phenyl)-ethyl]-4,5-dihydro-oxazol-2-ylamine,
(S)-4-(1-methyl-2-phenyl-ethyl)-4,5-dihydro-oxazol-2-ylamine,
(S)-4-[2-(2-fluoro-5-trifluoromethyl-phenyl)-ethyl]-4,5-dihydro-oxazol-2-ylamine,
(S)-4-[2-(3-fluoro-5-trifluoromethyl-phenyl)-ethyl]-4,5-dihydro-oxazol-2-ylamine,
(S)-4-[2-(2,5-bis-trifluoromethyl-phenyl)-ethyl]-4,5-dihydro-oxazol-2-ylamine,
(S)-4-[2-(4-chloro-phenyl)-butyl]-4,5-dihydro-oxazol-2-ylamine,
(S)-4-(2-phenyl-butyl)-4,5-dihydro-oxazol-2-ylamine,
(S)-4-[2-(4-trifluoromethyl-phenyl)-propyl]-4,5-di is Idro-oxazol-2-ylamine,
(S)-4-[2-(4-trifluoromethyl-phenyl)-butyl]-4,5-dihydro-oxazol-2-ylamine,
(S)-4-[2-(3-trifluoromethyl-phenyl)-propyl]-4,5-dihydro-oxazol-2-ylamine,
(S)-4-[2-(3-trifluoromethyl-phenyl)-butyl]-4,5-dihydro-oxazol-2-ylamine,
(S)-4-[2-(3,5-debtor-phenyl)-propyl]-4,5-dihydro-oxazol-2-ylamine,
(S)-4-[2-(3,5-debtor-phenyl)-butyl]-4,5-dihydro-oxazol-2-ylamine,
(S)-4-[2-(4-fluoro-phenyl)-butyl]-4,5-dihydro-oxazol-2-ylamine,
(S)-4-[2-(3,4-debtor-phenyl)-butyl]-4,5-dihydro-oxazol-2-ylamine,
(S)-4-[2-(2-fluoro-phenyl)-propyl]-4,5-dihydro-oxazol-2-ylamine,
(S)-4-[2-(3,4-dichloro-phenyl)-propyl]-4,5-dihydro-oxazol-2-ylamine,
(S)-4-[2-(3,4-dichloro-phenyl)-butyl]-4,5-dihydro-oxazol-2-ylamine,
(S)-4-[2-(2-fluoro-phenyl)-butyl]-4,5-dihydro-oxazol-2-ylamine,
(S)-4-[2-(2-chloro-phenyl)-ethyl]-4-methyl-4,5-dihydro-oxazol-2-ylamine,
(S)-4-[2-(3-chloro-phenyl)-ethyl]-4,5-dihydro-oxazol-2-ylamine,
(S)-4-[2-(4-chloro-phenyl)-ethyl]-4-methyl-4,5-dihydro-oxazol-2-ylamine,
(S)-4-[2-(3-chloro-phenyl)-ethyl]-4-methyl-4,5-dihydro-oxazol-2-ylamine,
(S)-4-[2-(4-fluoro-phenyl)-ethyl]-4-methyl-4,5-dihydro-oxazol-2-ylamine,
(S)-4-[2-(4-chloro-phenyl)-ethyl]-4,5-dihydro-oxazol-2-ylamine,
(S)-4-[2-(2-chloro-phenyl)-ethyl]-4,5-dihydro-oxazol-2-ylamine,
(S)-4-[2-(3-chloro-phenyl)-butyl]-4,5-dihydro-oxazol-2-ylamine,
(S)-4-((S)-2-phenyl-butyl)-4,5-dihydro-oxazol-2-ylamine,
(S)-4-((R)-2-phenyl-butyl)-4,5-dihydro-oxazol-2-ylamine,
(S)-4-[2-(2-chloro-6-fluoro-phenyl)-ethyl]-4,5-dihydro-oxazol-2-ylamine,
(S)-4-[2-(2,4-dichloro-phenyl)-ethyl]-4-methyl-4,5-dihydro-about Sasol-2-ylamine,
(S)-4-[2-(2-bromo-phenyl)-ethyl]-4,5-dihydro-oxazol-2-ylamine,
(S)-4-[2-(2,5-dichloro-phenyl)-ethyl]-4,5-dihydro-oxazol-2-ylamine,
(S)-4-[2-(3-fluoro-phenyl)-butyl]-4,5-dihydro-oxazol-2-ylamine,
(S)-4-[2-(3-chloro-2-fluoro-phenyl)-butyl]-4,5-dihydro-oxazol-2-ylamine,
(S)-4-[2-(3-chloro-4-fluoro-phenyl)-butyl]-4,5-dihydro-oxazol-2-ylamine,
(S)-4-[2-(3-chloro-5-fluoro-phenyl)-butyl]-4,5-dihydro-oxazol-2-ylamine or
(S)-4-[2-(5-chloro-2-fluoro-phenyl)-butyl]-4,5-dihydro-oxazol-2-ylamine.

15. The use of the compounds of formula I according to claim 1, where X represents co2and Y is phenyl.

16. The use of the compounds of formula I according to § 15, which is a
(S)-4-(4-fluoro-phenoxymethyl)-4,5-dihydro-oxazol-2-ylamine,
(S)-4-(4-chloro-phenoxymethyl)-4,5-dihydro-oxazol-2-ylamine,
(S)-4-(3,4-dichloro-phenoxymethyl)-4,5-dihydro-oxazol-2-ylamine,
(S)-4-(3,5-dichloro-phenoxymethyl)-4,5-dihydro-oxazol-2-ylamine,
(S)-4-(4-bromo-phenoxymethyl)-4,5-dihydro-oxazol-2-ylamine,
(S)-4-(3-chloro-phenoxymethyl)-4,5-dihydro-oxazol-2-ylamine,
(S)-4-(2,4-debtor-phenoxymethyl)-4,5-dihydro-oxazol-2-ylamine or
(S)-4-(2-fluoro-phenoxymethyl)-4,5-dihydro-oxazol-2-ylamine.

17. The use of the compounds of formula I according to claim 1, where X represents CH2OCHR and Y represents a phenyl, where the connection specified is a
(S)-4-benzoyloxymethyl-4,5-dihydro-oxazol-2-ylamine.

18. The use of the compounds of formula I according to claim 1, where X represents Soboh is -(CH 2)3and Y represents a phenyl, where these compounds are
(S)-4-(3-phenyl-propyl)-4,5-dihydro-oxazol-2-ylamine or
(R)-4-(3-phenyl-propyl)-4,5-dihydro-oxazol-2-ylamine.

19. The use of the compounds of formula I according to claim 1, where X represents-SCH2-, -S(O)2CH2- or-CH2SCH2and Y represents a phenyl, where these compounds are
(R)-4-phenylsulfanyl-4,5-dihydro-oxazol-2-ylamine,
(R)-4-benzosulfimide-4,5-dihydro-oxazol-2-ylamine,
(R)-4-benzylsulfamide-4,5-dihydro-oxazol-2-ylamine or
(R)-4-(4-chloro-phenylsulfonyl)-4,5-dihydro-oxazol-2-ylamine.

20. The use of the compounds of formula I according to claim 1, where X represents-CH2N(R)CH2-With3-6-cycloalkyl-CH2or SiRR'-CH2and Y represents phenyl, which is a
(S)-4-[1-(4-chloro-phenyl)-cyclopropylmethyl]-4,5-dihydro-oxazol-2-ylamine,
(S)-4-[1-(4-chloro-phenyl)-cyclobutylmethyl]-4,5-dihydro-oxazol-2-ylamine,
(S)-4-(1-phenyl-cyclopropylmethyl)-4,5-dihydro-oxazol-2-ylamine,
(S)-4-[(benzyl-ethyl-amino)-methyl]-4,5-dihydro-oxazol-2-ylamine or
(R)-4-[(dimethyl-phenyl-silanol)-methyl]-4,5-dihydro-oxazol-2-ylamine.

21. The use of the compounds of formula I according to claim 1, where X is as described in claim 1, and Y is naphthyl, pyridyl, cyclohexyl, 2,3-dihydrobenzo[1,4] dioxin or 1,2,3,4-tetrahedronal the'alene, which is a
(RS)-4-(2,3-dihydro-benzo[1,4]dioxin-6-yl)-4,5-dihydro-oxazol-2-ylamine,
(RS)-4-naphthalene-2-yl-4,5-dihydro-oxazol-2-ylamine,
(RS)-4-naphthalene-1-yl-4,5-dihydro-oxazol-2-ylamine,
(R)-4-naphthalene-1-ylmethyl-4,5-dihydro-oxazol-2-ylamine,
(S)-4-naphthalene-1-ylmethyl-4,5-dihydro-oxazol-2-ylamine,
(S)-4-naphthalene-2-ylmethyl-4,5-dihydro-oxazol-2-ylamine,
(RS)-4-(1,2,3,4-tetrahydro-naphthalene-2-yl)-4,5-dihydro-oxazol-2-ylamine,
(S)-4-naphthalene-2-yl-4,5-dihydro-oxazol-2-ylamine,
(S)-4-[2-(3-fluoro-pyridine-4-yl)-ethyl]-4,5-dihydro-oxazol-2-ylamine,
(S)-4-[2-(6-trifluoromethyl-pyridin-2-yl)-ethyl]-4,5-dihydro-oxazol-2-ylamine,
(S)-4-[2-(2-methyl-pyridin-4-yl)-ethyl]-4,5-dihydro-oxazol-2-ylamine or
(S)-4-(2-cyclohexyl-ethyl)-4,5-dihydro-oxazol-2-ylamine.

22. The compound of formula I-A according to the formula I according to claim 1
,
where R1represents a halogen atom, when n>1, the halogen atoms may be the same or different;
R2represents a hydrogen atom or a C1-7-alkyl;
n is 1, 2 or 3;
or a pharmaceutically acceptable salt accession acid, except 4-(4-bromo-phenyl)-4,5-dihydro-oxazol-2-ylamine.

23. The compound of formula I-A according to item 22, which is a
(S)-4-(2-chloro-phenyl)-4,5-dihydro-oxazol-2-ylamine,
(RS)-4-(4-chloro-phenyl)-4,5-dihydro-oxazol-2-ylamine,
(RS)-4-(2,4-debtor-phenyl)-4,5-dihydro-oxazol-2-ylamine, (S)-4-(2,3-debtor-phenyl)-4,5-dihydro-oxazol-2-ylamine,
(RS)-4-(3,4-dichlorophenyl)-4,5-dihydro-oxazol-2-ylamine,
(RS)-4-(2,5-debtor-phenyl)-4,5-dihydro-oxazol-2-ylamine,
(RS)-4-(2,3,4-Cryptor-phenyl)-4,5-dihydro-oxazol-2-ylamine,
(RS)-4-(3-chloro-2-fluoro-phenyl)-4,5-dihydro-oxazol-2-ylamine,
(RS)-4-(5-chloro-2-fluoro-phenyl)-4,5-dihydro-oxazol-2-ylamine,
(S)-4-(3-bromo-2,4-debtor-phenyl)-4,5-dihydro-oxazol-2-ylamine,
(S)-4-(2,4-debtor-phenyl)-4,5-dihydro-oxazol-2-ylamine,
(S)-4-(3,4-dichloro-phenyl)-4,5-dihydro-oxazol-2-ylamine,
(S)-4-(2,5-debtor-phenyl)-4,5-dihydro-oxazol-2-ylamine,
(S)-4-(4-bromo-phenyl)-4,5-dihydro-oxazol-2-ylamine,
(S)-4-(2,4,5-Cryptor-phenyl)-4,5-dihydro-oxazol-2-ylamine,
(S)-4-(3-chloro-2-fluoro-phenyl)-4,5-dihydro-oxazol-2-ylamine,
(S)-4-(2,3,5-Cryptor-phenyl)-4,5-dihydro-oxazol-2-ylamine,
(S)-4-(3,4-dichloro-phenyl)-4-methyl-4,5-dihydro-oxazol-2-ylamine,
(S)-4-(4-chloro-phenyl)-4-methyl-4,5-dihydro-oxazol-2-ylamine,
(S)-4-(3,4-debtor-phenyl)-4,5-dihydro-oxazol-2-ylamine,
(S)-4-(2,3-dichloro-phenyl)-4,5-dihydro-oxazol-2-ylamine,
(S)-4-(4-chloro-phenyl)-4,5-dihydro-oxazol-2-ylamine,
(S)-4-(3,4,5-Cryptor-phenyl)-4,5-dihydro-oxazol-2-ylamine,
(S)-4-(3-chloro-4-fluoro-phenyl)-4,5-dihydro-oxazol-2-ylamine,
(S)-4-(4-chloro-3-fluoro-phenyl)-4,5-dihydro-oxazol-2-ylamine,
(S)-4-(3,5-debtor-phenyl)-4,5-dihydro-oxazol-2-ylamine,
(S)-4-(3-chloro-5-fluoro-phenyl)-4,5-dihydro-oxazol-2-ylamine,
(S)-4-(2-chloro-phenyl)-4-methyl-4,5-dihydro-oxazol-2-ylamine,
(RS)-4-(3-chloro-phenyl)-4,5-dihydrooxazolo-2-ylamine,
(RS)-4-(3-bromo-phenyl)-4,5-dihydro-oxazol-2-ylamine,
(S)-4-(2,5-debtor-phenyl)-4-methyl-4,5-dihydro-oxazol-2-ylamine,
(RS)-4-(3-fluoro-phenyl)-4,5-dihydro-oxazol-2-ylamine,
(RS)-4-(3,5-dichloro-phenyl)-4,5-dihydro-oxazol-2-ylamine,
(+)-(S)-4-(5-chloro-2-fluoro-phenyl)-4,5-dihydro-oxazol-2-ylamine,
(+)-(S)-4-(3-chloro-phenyl)-4,5-dihydro-oxazol-2-ylamine,
(S)-4-(2-fluoro-phenyl)-4-methyl-4,5-dihydro-oxazol-2-ylamine,
(+)-(S)-4-(3-bromo-phenyl)-4,5-dihydro-oxazol-2-ylamine,
(+)-(S)-4-(3-fluoro-phenyl)-4,5-dihydro-oxazol-2-ylamine,
(+)-(S)-4-(3,5-dichloro-phenyl)-4,5-dihydro-oxazol-2-ylamine,
(S)-4-(2,4-debtor-phenyl)-4-methyl-4,5-dihydro-oxazol-2-ylamine,
(RS)-4-methyl-4-(2,3,5-Cryptor-phenyl)-4,5-dihydro-oxazol-2-ylamine,
(S)-4-(4-bromo-phenyl)-4-methyl-4,5-dihydro-oxazol-2-ylamine,
(RS)-4-(2,4-dichloro-phenyl)-4,5-dihydro-oxazol-2-ylamine,
(S)-4-(4-chloro-3-fluoro-phenyl)-4-methyl-4,5-dihydro-oxazol-2-ylamine,
(RS)-4-(2-bromo-phenyl)-4,5-dihydro-oxazol-2-ylamine,
(RS)-4-methyl-4-(2,4,5-Cryptor-phenyl)-4,5-dihydro-oxazol-2-ylamine,
(RS)-4-(4-bromo-3-fluoro-phenyl)-4,5-dihydro-oxazol-2-ylamine,
(RS)-4-(2,5-dichloro-phenyl)-4,5-dihydro-oxazol-2-ylamine,
(+)-(S)-4-(2-bromo-phenyl)-4,5-dihydro-oxazol-2-ylamine,
(S)-4-(3-chloro-5-fluoro-phenyl)-4-methyl-4,5-dihydro-oxazol-2-ylamine,
(RS)-4-methyl-4-(2,3,4-Cryptor-phenyl)-4,5-dihydro-oxazol-2-ylamine,
(S)-4-(5-chloro-2-fluoro-phenyl)-4-methyl-4,5-dihydro-oxazol-2-ylamine,
(RS)-4-methyl-4-(4-chloro-2,5-debtor-phenyl)-4,5-dihydro-oxazol-2-ylamine,
(RS)-4-methyl-4-(3,4,5-Cryptor-enyl)-4,5-dihydro-oxazol-2-ylamine,
(S)-4-(3-chloro-4-fluoro-phenyl)-4-methyl-4,5-dihydro-oxazol-2-ylamine,
(S)-4-(4-chloro-2,5-debtor-phenyl)-4-methyl-4,5-dihydro-oxazol-2-ylamine,
(RS)-4-(4-bromo-2-chloro-phenyl)-4,5-dihydro-oxazol-2-ylamine,
(RS)-4-(2,4-dichloro-phenyl)-4-methyl-4,5-dihydro-oxazol-2-ylamine,
(-)-(R)-4-(2,4-dichloro-phenyl)-4,5-dihydro-oxazol-2-ylamine,
(+)-(S)-4-(2,4-dichloro-phenyl)-4,5-dihydro-oxazol-2-ylamine,
(+)-(S)-4-(2,5-dichloro-phenyl)-4,5-dihydro-oxazol-2-ylamine,
(RS)-4-(2,5-dichloro-phenyl)-4-methyl-4,5-dihydro-oxazol-2-ylamine,
(+)-(S)-4-(2,3,4-Cryptor-phenyl)-4,5-dihydro-oxazol-2-ylamine,
(S)-4-methyl-4-(3,4,5-Cryptor-phenyl)-4,5-dihydro-oxazol-2-ylamine,
(RS)-4-(3-chloro-2-fluoro-phenyl)-4-methyl-4,5-dihydro-oxazol-2-ylamine,
(S)-4-(4-chloro-phenyl)-4-ethyl-4,5-dihydro-oxazol-2-ylamine,
(-)-(RS)-4-(4-bromo-2-chloro-phenyl)-4,5-dihydro-oxazol-2-ylamine,
(+)-(S)-4-(4-bromo-2-chloro-phenyl)-4,5-dihydro-oxazol-2-ylamine,
(RS)-4-(2-chloro-4-fluoro-phenyl)-4-methyl-4,5-dihydro-oxazol-2-ylamine,
(+)-(S)-4-(4-bromo-3-fluoro-phenyl)-4,5-dihydro-oxazol-2-ylamine,
(RS)-4-(4-bromo-3-chloro-phenyl)-4,5-dihydro-oxazol-2-ylamine,
(S)-4-(3,4-dichloro-phenyl)-4-ethyl-4,5-dihydro-oxazol-2-ylamine,
(+)-(S)-4-(4-bromo-3-chloro-phenyl)-4,5-dihydro-oxazol-2-ylamine,
(RS)-4-(4-bromo-2-fluoro-phenyl)-4,5-dihydro-oxazol-2-ylamine or
(S)-4-(4-bromo-2-fluoro-phenyl)-4,5-dihydro-oxazol-2-ylamine.

24. The compound of formula 1 according to the formula I according to claim 1,

where R1represents CH3, CF3The co , OCF3or och2is phenyl;
R2represents a hydrogen atom or a C1-7-alkyl;
n is 1, 2 or 3;
or a pharmaceutically acceptable salt accession acid, except
4-(4-trifluoromethyl-phenyl)4,5-dihydro-oxazol-2-ylamine,
4-(4-methoxy-phenyl)4,5-dihydro-oxazol-2-ylamine and
4-(3,4-dimethoxy-phenyl)4,5-dihydro-oxazol-2-ylamine.

25. The compound of formula I In point 24, which represents
(RS)-4-(2-trifluoromethyl-phenyl)-4,5-dihydro-oxazol-2-ylamine,
(RS)-4-ortho-tolyl-4,5-dihydro-oxazol-2-ylamine,
(RS)-4-(4-triptoreline-phenyl)-4,5-dihydro-oxazol-2-ylamine,
(RS)-4-(4-methoxy-3-methyl-phenyl)-4,5-dihydro-oxazol-2-ylamine,
(S)-4-ortho-tolyl-4,5-dihydro-oxazol-2-ylamine,
(RS)-4-(4-benzyloxy-phenyl)-4,5-dihydro-oxazol-2-ylamine,
(S)-4-(2-trifluoromethyl-phenyl)-4,5-dihydro-oxazol-2-ylamine,
(S)-4-(4-methoxy-3-methyl-phenyl)-4,5-dihydro-oxazol-2-ylamine,
(S)-4-methyl-4-(4-trifluoromethyl-phenyl)-4,5-dihydro-oxazol-2-ylamine,
(S)-4-(3-trifluoromethyl-phenyl)-4,5-dihydro-oxazol-2-ylamine,
(S)-4-methyl-4-para-tolyl-4,5-dihydro-oxazol-2-ylamine,
(S)-4-methyl-4-(3-trifluoromethyl-phenyl)-4,5-dihydro-oxazol-2-ylamine,
(RS)-4-(4-methoxy-2-trifluoromethyl-phenyl)-4,5-dihydro-oxazol-2-ylamine,
(+)-(S)-4-(4-methoxy-2-trifluoromethyl-phenyl)-4,5-dihydro-oxazol-2-ylamine.

26. The compound of formula I-C according to the formula I according to claim 1

where R2PR is dstanley a hydrogen atom or a C 1-7-alkyl, or a pharmaceutically acceptable salt accession acid.

27. The compound of formula I-C in p, which is a
(RS)-4-biphenyl-4-yl-4,5-dihydro-oxazol-2-ylamine,
(S)-4-biphenyl-4-yl-4,5-dihydro-oxazol-2-ylamine or
(RS)-4-(4'-chloro-biphenyl-4-yl)-4,5-dihydro-oxazol-2-ylamine.

28. The compound of formula I-D according to the formula I according to claim 1

where R1represents a halogen atom and CF3, a halogen atom and CH3, a halogen atom and C3-6-cycloalkyl or represents a halogen atom and co3;
R2represents a hydrogen atom or a C1-7-alkyl;
n is 1, 2 or 3;
or a pharmaceutically acceptable salt accession acid.

29. The compound of formula I-D p, where these compounds are
(RS)-4-(3-chloro-4-methoxyphenyl)-4,5-dihydro-oxazol-2-ylamine,
(S)-4-(3-chloro-4-methoxy-phenyl)-4,5-dihydro-oxazol-2-ylamine,
(S)-4-(2-fluoro-4-trifluoromethyl-phenyl)-4-methyl-4,5-dihydro-oxazol-2-ylamine,
(RS)-4-(4-fluoro-2-trifluoromethyl-phenyl)-4,5-dihydro-oxazol-2-ylamine,
(RS)-4-(5-chloro-2-trifluoromethyl-phenyl)-4,5-dihydro-oxazol-2-ylamine,
(RS)-4-(4-chloro-2-trifluoromethyl-phenyl)-4,5-dihydro-oxazol-2-ylamine,
(RS)-4-(4,5-dichloro-2-trifluoromethyl-phenyl)-4,5-dihydro-oxazol-2-ylamine,
(+)-(S)-4-(4-chloro-2-trifluoromethyl-phenyl)-4,5-dihydro-oxazol-2-ylamine,
(+)-(S)-4-(4,5-dichloro-2-trifluoromethyl-FeNi is)-4,5-dihydro-oxazol-2-ylamine,
(-)-(R)-4-(4,5-dichloro-2-trifluoromethyl-phenyl)-4,5-dihydro-oxazol-2-ylamine,
(+)-(S)-4-(4-fluoro-2-trifluoromethyl-phenyl)-4,5-dihydro-oxazol-2-ylamine,
(RS)-4-(5-fluoro-2-trifluoromethyl-phenyl)-4,5-dihydro-oxazol-2-ylamine,
(RS)-4-(5-fluoro-2-methyl-phenyl)-4,5-dihydro-oxazol-2-ylamine,
(+)-(S)-4-(5-fluoro-2-trifluoromethyl-phenyl)-4,5-dihydro-oxazol-2-ylamine,
(RS)-4-(4-chloro-3-methyl-phenyl)-4-methyl-4,5-dihydro-oxazol-2-ylamine,
(RS)-4-(5-chloro-2-methyl-phenyl)-4,5-dihydro-oxazol-2-ylamine,
(RS)-4-(4-chloro-2-fluoro-5-methyl-phenyl)-4-methyl-4,5-dihydro-oxazol-2-ylamine,
(S)-4-(4-chloro-3-methyl-phenyl)-4-methyl-4,5-dihydro-oxazol-2-ylamine,
(RS)-4-(4-bromo-2-trifluoromethyl-phenyl)-4,5-dihydro-oxazol-2-ylamine,
(S)-4-(4-chloro-2-fluoro-5-methyl-phenyl)-4-methyl-4,5-dihydro-oxazol-2-ylamine,
(+)-(S)-4-(5-chloro-2-methyl-phenyl)-4,5-dihydro-oxazol-2-ylamine,
(RS)-4-(4-fluoro-2-methyl-phenyl)-4,5-dihydro-oxazol-2-ylamine,
(+)-(S)-4-(4-bromo-2-trifluoromethyl-phenyl)-4,5-dihydro-oxazol-2-ylamine,
(+)-(S)-4-(5-chloro-2-trifluoromethyl-phenyl)-4,5-dihydro-oxazol-2-ylamine,
(RS)-4-(4-chloro-2-ethyl-phenyl)-4,5-dihydro-oxazol-2-ylamine,
(+)-(S)-4-(4-fluoro-2-methyl-phenyl)-4,5-dihydro-oxazol-2-ylamine,
(RS)-4-(3-chloro-4-methyl-phenyl)-4,5-dihydro-oxazol-2-ylamine,
(RS)-4-(4-chloro-2-cyclopropyl-phenyl)-4,5-dihydro-oxazol-2-ylamine,
(S)-4-(4-chloro-2-ethyl-phenyl)-4,5-dihydro-oxazol-2-ylamine,
(RS)-4-(3-fluoro-2-methyl-phenyl)-4,5-dihydro-oxazol-2-ylamine,
(S)-4-(4-chloro-2-cyclopropyl-phenyl)-4,5-dihydro-oxazol-2-ylamine,
(RS)-4(3-fluoro-2-trifluoromethyl-phenyl)-4,5-dihydro-oxazol-2-ylamine or
(S)-4-(3-chloro-4-methyl-phenyl)-4,5-dihydro-oxazol-2-ylamine.

30. The compound of formula 1-E according to the formula I according to claim 1

where R1represents a halogen atom, CF3or CH3,
R2represents a hydrogen atom or a C1-7-alkyl;
R can be a C1-7-alkyl or C1-7-alkyl, substituted by a halogen atom;
n is 1 or 2;
or a pharmaceutically acceptable salt accession acid.

31. The compound of formula I-F according to the formula I according to claim 1

where R1represents a hydrogen atom, a C1-7-alkyl, C1-7-alkoxy, C1-7-alkyl, substituted by a halogen atom, a C1-7-alkoxy substituted by halogen atom, or represents a halogen atom, where n>1 these substituents may be the same or different;
R/R' independently of one another can represent a hydrogen atom, a C1-7-alkyl or C1-7-alkyl substituted by halogen atom, provided that when R1represents a hydrogen atom or a C1-7-alkoxy, R and R' are not simultaneously hydrogen atoms;
R2represents a hydrogen atom or a C1-7-alkyl;
n is 0, 1, 2 or 3;
or a pharmaceutically acceptable salt accession acid, except
4-phenethyl-4,5-dihydro-oxazol-2-Il, 4-[2-(2-methoxy-phenyl)-ethyl]-4,5-digitar-oxazol-2-Il,
4-[2-(4-methoxy-phenyl)-ethyl]-4,5-dihydro-oxazol-2-yl and
4-[2-(3,4-dimethoxy-phenyl)-ethyl]-4,5-dihydro-oxazol-2-yl.

32. The compound of formula I-F in p, which is a
(S)-4-[2-(4-fluoro-phenyl)-ethyl]-4,5-dihydro-oxazol-2-ylamine,
(S)-4-[2-(4-fluoro-3-methoxy-phenyl)-ethyl]-4,5-dihydro-oxazol-2-ylamine,
((S)-4-[2-(2,4-debtor-phenyl)-ethyl]-4,5-dihydro-oxazol-2-ylamine,
(S)-4-[2-(3,4-debtor-phenyl)-ethyl]-4,5-dihydro-oxazol-2-ylamine,
(S)-4-[2-(2-trifluoromethyl-phenyl)-ethyl]-4,5-dihydro-oxazol-2-ylamine,
(S)-4-[2-(2-fluoro-phenyl)-ethyl]-4,5-dihydro-oxazol-2-ylamine,
(S)-4-[2-(3-fluoro-phenyl)-ethyl]-4,5-dihydro-oxazol-2-ylamine,
(S)-4-[2-(3,5-debtor-phenyl)-ethyl]-4,5-dihydro-oxazol-2-ylamine,
(S)-4-(2-ortho-tolyl-ethyl)-4,5-dihydro-oxazol-2-ylamine,
(S)-4-(2-meta-tolyl-ethyl)-4,5-dihydro-oxazol-2-ylamine,
(S)-4-(2-para-tolyl-ethyl)-4,5-dihydro-oxazol-2-ylamine,
(S)-4-[2-(4-trifluoromethyl-phenyl)-ethyl]-4,5-dihydro-oxazol-2-ylamine,
(S)-4-[2-(3-trifluoromethyl-phenyl)-ethyl]-4,5-dihydro-oxazol-2-ylamine,
(R)-4-[2-(3,4-dichloro-phenyl)-ethyl]-4,5-dihydro-oxazol-2-ylamine,
(S)-4-[2-(3,4-dichloro-phenyl)-ethyl]-4,5-dihydro-oxazol-2-ylamine,
(S)-4-[2-(4-chloro-2-fluoro-phenyl)-ethyl]-4,5-dihydro-oxazol-2-ylamine,
(S)-4-[2-(4-fluoro-3-trifluoromethyl-phenyl)-ethyl]-4,5-dihydro-oxazol-2-ylamine,
(S)-4-[2-(3-fluoro-4-trifluoromethyl-phenyl)-ethyl]-4,5-dihydro-oxazol-2-ylamine,
(S)-4-[2-(3,5-dichloro-phenyl)-ethyl]-4,5-dihydro-oxazol-ylamine,
(S)-4-[2-(2-chloro-4-fluoro-phenyl)-ethyl]-4,5-dihydro-oxazol-2-ylamine,
(S)-4-[2-(4-fluoro-3-methyl-phenyl)-ethyl]-4,5-dihydro-oxazol-2-ylamine,
(S)-4-{2-[3-(1,1,2,2-titrator-ethoxy)-phenyl]-ethyl}-4,5-dihydro-oxazol-2-ylamine,
(S)-4-[2-(2-fluoro-3-trifluoromethyl-phenyl)-ethyl]-4,5-dihydro-oxazol-2-ylamine,
(S)-4-[2-(3-bromo-phenyl)-ethyl]-4,5-dihydro-oxazol-2-ylamine,
(S)-4-[2-(4-chloro-3-trifluoromethyl-phenyl)-ethyl]-4,5-dihydro-oxazol-2-ylamine,
(S)-4-[2-(3-fluoro-4-triptoreline-phenyl)-ethyl]-4,5-dihydro-oxazol-2-ylamine,
(S)-4-[2-(4-fluoro-3-triptoreline-phenyl)-ethyl]-4,5-dihydro-oxazol-2-ylamine,
(S)-4-[2-(2,3-dichloro-phenyl)-ethyl]-4,5-dihydro-oxazol-2-ylamine,
(S)-4-[2-(3-chloro-4-triptoreline-phenyl)-ethyl]-4,5-dihydro-oxazol-2-ylamine,
(S)-4-[2-(2-chloro-3-trifluoromethyl-phenyl)-ethyl]-4,5-dihydro-oxazol-2-ylamine,
(S)-4-(1-methyl-2-phenyl-ethyl)-4,5-dihydro-oxazol-2-ylamine,
(S)-4-[2-(2-fluoro-5-trifluoromethyl-phenyl)-ethyl]-4,5-dihydro-oxazol-2-ylamine,
(S)-4-[2-(3-fluoro-5-trifluoromethyl-phenyl)-ethyl]-4,5-dihydro-oxazol-2-ylamine,
(S)-4-[2-(2,5-bis-trifluoromethyl-phenyl)-ethyl]-4,5-dihydro-oxazol-2-ylamine,
(S)-4-[2-(4-chloro-phenyl)-butyl]-4,5-dihydro-oxazol-2-ylamine,
(S)-4-(2-phenyl-butyl)-4,5-dihydro-oxazol-2-ylamine,
(S)-4-[2-(4-trifluoromethyl-phenyl)-propyl]-4,5-dihydro-oxazol-2-ylamine,
(S)-4-[2-(4-trifluoromethyl-phenyl)-butyl]-4,5-dihydro-oxazol-2-ylamine,
(S)-4-[2-(3-trifluoromethyl-phenyl)-propyl]-4,5-dihydro-oxazol-2-ylamine,
(S)-4-[2-(3-trifluoromethyl-phenyl)-butyl]-4,5-Digi the Rho-oxazol-2-ylamine,
(S)-4-[2-(3,5-debtor-phenyl)-propyl]-4,5-dihydro-oxazol-2-ylamine,
(S)-4-[2-(3,5-debtor-phenyl)-butyl]-4,5-dihydro-oxazol-2-ylamine,
(S)-4-[2-(4-fluoro-phenyl)-butyl]-4,5-dihydro-oxazol-2-ylamine,
(S)-4-[2-(3,4-debtor-phenyl)-butyl]-4,5-dihydro-oxazol-2-ylamine,
(S)-4-[2-(2-fluoro-phenyl)-propyl]-4,5-dihydro-oxazol-2-ylamine,
(S)-4-[2-(3,4-dichloro-phenyl)-propyl]-4,5-dihydro-oxazol-2-ylamine,
(S)-4-[2-(3,4-dichloro-phenyl)-butyl]-4,5-dihydro-oxazol-2-ylamine,
(S)-4-[2-(2-fluoro-phenyl)-butyl]-4,5-dihydro-oxazol-2-ylamine,
(S)-4-[2-(2-chloro-phenyl)-ethyl]-4-methyl-4,5-dihydro-oxazol-2-ylamine,
(S)-4-[2-(3-chloro-phenyl)-ethyl]-4,5-dihydro-oxazol-2-ylamine,
(S)-4-[2-(4-chloro-phenyl)-ethyl]-4-methyl-4,5-dihydro-oxazol-2-ylamine,
(S)-4-[2-(3-chloro-phenyl)-ethyl]-4-methyl-4,5-dihydro-oxazol-2-ylamine,
(S)-4-[2-(4-fluoro-phenyl)-ethyl]-4-methyl-4,5-dihydro-oxazol-2-ylamine,
(S)-4-[2-(4-chloro-phenyl)-ethyl]-4,5-dihydro-oxazol-2-ylamine,
(S)-4-[2-(2-chloro-phenyl)-ethyl]-4,5-dihydro-oxazol-2-ylamine,
(S)-4-[2-(3-chloro-phenyl)-butyl]-4,5-dihydro-oxazol-2-ylamine,
(S)-4-((S)-2-phenyl-butyl)-4,5-dihydro-oxazol-2-ylamine,
(S)-4-((R)-2-phenyl-butyl)-4,5-dihydro-oxazol-2-ylamine,
(S)-4-[2-(2-chloro-6-fluoro-phenyl)-ethyl]-4,5-dihydro-oxazol-2-ylamine,
(S)-4-[2-(2,4-dichloro-phenyl)-ethyl]-4-methyl-4,5-dihydro-oxazol-2-ylamine,
(S)-4-[2-(2-bromo-phenyl)-ethyl]-4,5-dihydro-oxazol-2-ylamine,
(S)-4-[2-(2,5-dichloro-phenyl)-ethyl]-4,5-dihydro-oxazol-2-ylamine,
(S)-4-[2-(3-fluoro-phenyl)-butyl]-4,5-dihydro-oxazol-2-ylamine,
(S)-4-[2-(3-the ers-2-fluoro-phenyl)-butyl]-4,5-dihydro-oxazol-2-ylamine,
(S)-4-[2-(3-chloro-4-fluoro-phenyl)-butyl]-4,5-dihydro-oxazol-2-ylamine,
(S)-4-[2-(3-chloro-5-fluoro-phenyl)-butyl]-4,5-dihydro-oxazol-2-ylamine or
(S)-4-[2-(5-chloro-2-fluoro-phenyl)-butyl]-4,5-dihydro-oxazol-2-ylamine.

33. The compound of formula I-G according to the formula I according to claim 1

where R1represents a C1-7-alkyl or C1-7-alkyl, substituted by a halogen atom, where n>1 these substituents may be the same or different;
R2represents a hydrogen atom or a C1-7-alkyl;
n is 0, 1, 2 or 3;
or a pharmaceutically acceptable salt accession acid, except 4-phenoxy-methyl-4,5-dihydro-oxazol-2-ylamine.

34. The compound of formula I-H according to the formula I according to claim 1

where R1represents a halogen atom;
n is 0 or 1;
or a pharmaceutically acceptable salt accession acid, except 4-benzoyloxymethyl-4,5-dihydro-oxazol-2-ylamine.

35. The compound of the formula I

where X represents -(CH2)3-, Y is phenyl and the other radicals such as defined in claim 1.

36. The compound of formula I according p, which is a
(S)-4-(3-phenyl-propyl)-4,5-dihydro-oxazol-2-ylamine or
(R)-4-(3-phenyl-propyl)-4,5-dihydro-oxazol-2-ylamine.

37. The connection f is rmula I

where I X is a-SCH2-, -S(O)2CH2-, -CH2S(O)2CH2- or-CH2SCH2-, Y is phenyl and the other radicals such as defined in claim 1.

38. The compound of formula I according to clause 37, which is a
(R)-4-phenylsulfanyl-4,5-dihydro-oxazol-2-ylamine,
(R)-4-benzosulfimide-4,5-dihydro-oxazol-2-ylamine,
(R)-4-benzylsulfamide-4,5-dihydro-oxazol-2-ylamine or
(R)-4-(4-chloro-phenylsulfonyl)-4,5-dihydro-oxazol-2-ylamine.

39. The compound of the formula I

where X represents-CH2N(R)CH2-With3-6-cycloalkyl-CH2or SiRR'-CH2-, Y is phenyl and the other radicals such as defined in claim 1.

40. The compound of formula I according to § 39, which is a
(S)-4-[1-(4-chloro-phenyl)-cyclopropylmethyl]-4,5-dihydro-oxazol-2-ylamine,
(S)-4-[1-(4-chloro-phenyl)-cyclobutylmethyl]-4,5-dihydro-oxazol-2-ylamine,
(S)-4-(1-phenyl-cyclopropylmethyl)-4,5-dihydro-oxazol-2-ylamine,
(S)-4-[(benzyl-ethyl-amino)-methyl]-4,5-dihydro-oxazol-2-ylamine or
(R)-4-[(dimethyl-phenyl-silanol)-methyl]-4,5-dihydro-oxazol-2-ylamine.

41. The compound of the formula I

where X is as described in claim 1, Y is naphthyl, pyridyl, cyclohexyl, 2,3-dihydrobenzo[1,4]is iaxin or 1,2,3,4-tetrahydronaphthalen, except 4-naphthalene-2-yl-4,5-dihydro-oxazol-2-ylamine, and the values of other radicals such as defined in claim 1.

42. The compound of formula I according to paragraph 41, which is a
(RS)-4-(2,3-dihydro-benzo[1,4]dioxin-6-yl)-4,5-dihydro-oxazol-2-ylamine,
(RS)-4-naphthalene-1-yl-4,5-dihydro-oxazol-2-ylamine,
(R)-4-naphthalene-1-ylmethyl-4,5-dihydro-oxazol-2-ylamine,
(S)-4-naphthalene-1-ylmethyl-4,5-dihydro-oxazol-2-ylamine,
(S)-4-naphthalene-2-ylmethyl-4,5-dihydro-oxazol-2-ylamine,
(RS)-4-(1,2,3,4-tetrahydro-naphthalene-2-yl)-4,5-dihydro-oxazol-2-ylamine,
(S)-4-[2-(3-fluoro-pyridine-4-yl)-ethyl]-4,5-dihydro-oxazol-2-ylamine,
(S)-4-[2-(6-trifluoromethyl-pyridin-2-yl)-ethyl]-4,5-dihydro-oxazol-2-ylamine,
(S)-4-[2-(2-methyl-pyridin-4-yl)-ethyl]-4,5-dihydro-oxazol-2-ylamine or
(S)-4-(2-cyclohexyl-ethyl)-4,5-dihydro-oxazol-2-ylamine.

43. Pharmaceutical composition for treatment of diseases associated with the biological function of the receptor associated with the trace amines containing one of the compounds according PP-42:
(S)-4-(2-chloro-phenyl)-4,5-dihydro-oxazol-2-ylamine,
(RS)-4-(4-chloro-phenyl)-4,5-dihydro-oxazol-2-ylamine,
(RS)-4-(2,4-debtor-phenyl)-4,5-dihydro-oxazol-2-ylamine,
(S)-4-(2,3-debtor-phenyl)-4,5-dihydro-oxazol-2-ylamine,
(RS)-4-(3,4-dichlorophenyl)-4,5-dihydro-oxazol-2-ylamine,
(RS)-4-(2,5-debtor-phenyl)-4,5-dihydro-oxazol-2-ylamine,
(RS)-4-(2,3,4-Cryptor-phenyl)-4,5-dihydro-oxazol-2-ylamine,
(RS)-4-(3-chloro-2-fluoro-Fe who yl)-4,5-dihydro-oxazol-2-ylamine,
(RS)-4-(5-chloro-2-fluoro-phenyl)-4,5-dihydro-oxazol-2-ylamine,
(S)-4-(3-bromo-2,4-debtor-phenyl)-4,5-dihydro-oxazol-2-ylamine,
(S)-4-(2,4-debtor-phenyl)-4,5-dihydro-oxazol-2-ylamine,
(S)-4-(3,4-dichloro-phenyl)-4,5-dihydro-oxazol-2-ylamine,
(S)-4-(2,5-debtor-phenyl)-4,5-dihydro-oxazol-2-ylamine,
(S)-4-(4-bromo-phenyl)-4,5-dihydro-oxazol-2-ylamine,
(S)-4-(2,4,5-Cryptor-phenyl)-4,5-dihydro-oxazol-2-ylamine,
(S)-4-(3-chloro-2-fluoro-phenyl)-4,5-dihydro-oxazol-2-ylamine,
(S)-4-(2,3,5-Cryptor-phenyl)-4,5-dihydro-oxazol-2-ylamine,
(S)-4-(3,4-dichloro-phenyl)-4-methyl-4,5-dihydro-oxazol-2-ylamine,
(S)-4-(4-chloro-phenyl)-4-methyl-4,5-dihydro-oxazol-2-ylamine,
(S)-4-(3,4-debtor-phenyl)-4,5-dihydro-oxazol-2-ylamine,
(S)-4-(2,3-dichloro-phenyl)-4,5-dihydro-oxazol-2-ylamine,
(S)-4-(4-chloro-phenyl)-4,5-dihydro-oxazol-2-ylamine,
(S)-4-(3,4,5-Cryptor-phenyl)-4,5-dihydro-oxazol-2-ylamine,
(S)-4-(3-chloro-4-fluoro-phenyl)-4,5-dihydro-oxazol-2-ylamine,
(S)-4-(4-chloro-3-fluoro-phenyl)-4,5-dihydro-oxazol-2-ylamine,
(S)-4-(3,5-debtor-phenyl)-4,5-dihydro-oxazol-2-ylamine,
(S)-4-(3-chloro-5-fluoro-phenyl)-4,5-dihydro-oxazol-2-ylamine,
(S)-4-(2-chloro-phenyl)-4-methyl-4,5-dihydro-oxazol-2-ylamine,
(RS)-4-(3-chloro-phenyl)-4,5-dihydro-oxazol-2-ylamine,
(RS)-4-(3-bromo-phenyl)-4,5-dihydro-oxazol-2-ylamine,
(S)-4-(2,5-debtor-phenyl)-4-methyl-4,5-dihydro-oxazol-2-ylamine,
(RS)-4-(3-fluoro-phenyl)-4,5-dihydro-oxazol-2-ylamine,
(RS)-4-(3,5-dichloro-phenyl)-4,5-dihydro-oxazol-2-ylamine,
(+)-(S)-4-(5-chloro-2-fluoro-phenyl)-4,5-dihydr the-oxazol-2-ylamine,
(+)-(S)-4-(3-chloro-phenyl)-4,5-dihydro-oxazol-2-ylamine,
(S)-4-(2-fluoro-phenyl)-4-methyl-4,5-dihydro-oxazol-2-ylamine,
(+)-(S)-4-(3-bromo-phenyl)-4,5-dihydro-oxazol-2-ylamine,
(+)-(S)-4-(3-fluoro-phenyl)-4,5-dihydro-oxazol-2-ylamine,
(+)-(S)-4-(3,5-dichloro-phenyl)-4,5-dihydro-oxazol-2-ylamine,
(S)-4-(2,4-debtor-phenyl)-4-methyl-4,5-dihydro-oxazol-2-ylamine,
(RS)-4-methyl-4-(2,3,5-Cryptor-phenyl)-4,5-dihydro-oxazol-2-ylamine,
(S)-4-(4-bromo-phenyl)-4-methyl-4,5-dihydro-oxazol-2-ylamine,
(RS)-4-(2,4-dichloro-phenyl)-4,5-dihydro-oxazol-2-ylamine,
(S)-4-(4-chloro-3-fluoro-phenyl)-4-methyl-4,5-dihydro-oxazol-2-ylamine,
(RS)-4-(2-bromo-phenyl)-4,5-dihydro-oxazol-2-ylamine,
(RS)-4-methyl-4-(2,4,5-Cryptor-phenyl)-4,5-dihydro-oxazol-2-ylamine,
(RS)-4-(4-bromo-3-fluoro-phenyl)-4,5-dihydro-oxazol-2-ylamine,
(RS)-4-(2,5-dichloro-phenyl)-4,5-dihydro-oxazol-2-ylamine,
(+)-(S)-4-(2-bromo-phenyl)-4,5-dihydro-oxazol-2-ylamine,
(S)-4-(3-chloro-5-fluoro-phenyl)-4-methyl-4,5-dihydro-oxazol-2-ylamine,
(RS)-4-methyl-4-(2,3,4-Cryptor-phenyl)-4,5-dihydro-oxazol-2-ylamine,
(S)-4-(5-chloro-2-fluoro-phenyl)-4-methyl-4,5-dihydro-oxazol-2-ylamine,
(RS)-4-methyl-4-(4-chloro-2,5-debtor-phenyl)-4,5-dihydro-oxazol-2-ylamine,
(RS)-4-methyl-4-(3,4,5-Cryptor-phenyl)-4,5-dihydro-oxazol-2-ylamine,
(S)-4-(3-chloro-4-fluoro-phenyl)-4-methyl-4,5-dihydro-oxazol-2-ylamine,
(S)-4-(4-chloro-2,5-debtor-phenyl)-4-methyl-4,5-dihydro-oxazol-2-ylamine,
(RS)-4-(4-bromo-2-chloro-phenyl)-4,5-dihydro-oxazol-2-ylamine,
(RS)-4-(2,4-dichloro-phenyl)-4-methyl-4,5-dihydro-oxazo the-2-ylamine,
(-)-(R)-4-(2,4-dichloro-phenyl)-4,5-dihydro-oxazol-2-ylamine,
(+)-(S)-4-(2,4-dichloro-phenyl)-4,5-dihydro-oxazol-2-ylamine,
(+)-(S)-4-(2,5-dichloro-phenyl)-4,5-dihydro-oxazol-2-ylamine,
(RS)-4-(2,5-dichloro-phenyl)-4-methyl-4,5-dihydro-oxazol-2-ylamine,
(+)-(S)-4-(2,3,4-Cryptor-phenyl)-4,5-dihydro-oxazol-2-ylamine,
(S)-4-methyl-4-(3,4,5-Cryptor-phenyl)-4,5-dihydro-oxazol-2-ylamine,
(RS)-4-(3-chloro-2-fluoro-phenyl)-4-methyl-4,5-dihydro-oxazol-2-ylamine,
(S)-4-(4-chloro-phenyl)-4-ethyl-4,5-dihydro-oxazol-2-ylamine,
(-)-(R)-4-(4-bromo-2-chloro-phenyl)-4,5-dihydro-oxazol-2-ylamine,
(+)-(R)-4-(4-bromo-2-chloro-phenyl)-4,5-dihydro-oxazol-2-ylamine,
(RS)-4-(2-chloro-4-fluoro-phenyl)-4-methyl-4,5-dihydro-oxazol-2-ylamine,
(+)-(S)-4-(4-bromo-3-fluoro-phenyl)-4,5-dihydro-oxazol-2-ylamine,
(RS-4-(4-bromo-3-chloro-phenyl)-4,5-dihydro-oxazol-2-ylamine,
(S)-4-(3,4-dichloro-phenyl)-4-ethyl-4,5-dihydro-oxazol-2-ylamine,
(+)-(S)-4-(4-bromo-3-chloro-phenyl)-4,5-dihydro-oxazol-2-ylamine,
(RS)-4-(4-bromo-2-fluoro-phenyl)-4,5-dihydro-oxazol-2-ylamine,
(S)-4-(4-bromo-2-fluoro-phenyl)-4,5-dihydro-oxazol-2-ylamine,
(RS)-4-(2-trifluoromethyl-phenyl)-4,5-dihydro-oxazol-2-ylamine,
(RS)-4-ortho-tolyl-4,5-dihydro-oxazol-2-ylamine,
(RS)-4-(4-triptoreline-phenyl)-4,5-dihydro-oxazol-2-ylamine,
(RS)-4-(4-methoxy-3-methyl-phenyl)-4,5-dihydro-oxazol-2-ylamine,
(S)-4-ortho-tolyl-4,5-dihydro-oxazol-2-ylamine,
(RS)-4-(4-benzyloxy-phenyl)-4,5-dihydro-oxazol-2-ylamine,
(S)-4-(2-trifluoromethyl-phenyl)-4,5-dihydro-oxazol-2-ylamine,
(S)-4-(4-labels and-3-methyl-phenyl)-4,5-dihydro-oxazol-2-ylamine,
(S)-4-methyl-4-(4-trifluoromethyl-phenyl)-4,5-dihydro-oxazol-2-ylamine,
(S)-4-(3-trifluoromethyl-phenyl)-4,5-dihydro-oxazol-2-ylamine,
(S)-4-methyl-4-para-tolyl-4,5-dihydro-oxazol-2-ylamine,
(S)-4-methyl-4-(3-trifluoromethyl-phenyl)-4,5-dihydro-oxazol-2-ylamine,
(RS)-4-(4-methoxy-2-trifluoromethyl-phenyl)-4,5-dihydro-oxazol-2-ylamine,
(+)-(S)-4-(4-methoxy-2-trifluoromethyl-phenyl)-4,5-dihydro-oxazol-2-ylamine,
(RS)-4-biphenyl-4-yl-4,5-dihydro-oxazol-2-ylamine,
(S)-4-biphenyl-4-yl-4,5-dihydro-oxazol-2-ylamine,
(RS)-4-(4'-chloro-biphenyl-4-yl)-4,5-dihydro-oxazol-2-ylamine,
(RS)-4-(3-chloro-4-methoxyphenyl)-4,5-dihydro-oxazol-2-ylamine,
(S)-4-(3-chloro-4-methoxy-phenyl)-4,5-dihydro-oxazol-2-ylamine,
(S)-4-(2-fluoro-4-trifluoromethyl-phenyl)-4-methyl-4,5-dihydro-oxazol-2-ylamine,
(RS)-4-(4-fluoro-2-trifluoromethyl-phenyl)-4,5-dihydro-oxazol-2-ylamine,
(RS)-4-(5-chloro-2-trifluoromethyl-phenyl)-4,5-dihydro-oxazol-2-ylamine,
(RS)-4-(4-chloro-2-trifluoromethyl-phenyl)-4,5-dihydro-oxazol-2-ylamine,
(RS)-4-(4,5-dichloro-2-trifluoromethyl-phenyl)-4,5-dihydro-oxazol-2-ylamine,
(+)-(S)-4-(4-chloro-2-trifluoromethyl-phenyl)-4,5-dihydro-oxazol-2-ylamine,
(+)-(S)-4-(4,5-dichloro-2-trifluoromethyl-phenyl)-4,5-dihydro-oxazol-2-ylamine,
(-)-(R)-4-(4,5-dichloro-2-trifluoromethyl-phenyl)-4,5-dihydro-oxazol-2-ylamine,
(+)-(S)-4-(4-fluoro-2-trifluoromethyl-phenyl)-4,5-dihydro-oxazol-2-ylamine,
(RS)-4-(5-fluoro-2-trifluoromethyl-phenyl)-4,5-dihydro-oxazol-2-yl amine,
(RS)-4-(5-fluoro-2-methyl-phenyl)-4,5-dihydro-oxazol-2-ylamine,br/> (+)-(S)-4-(5-fluoro-2-trifluoromethyl-phenyl)-4,5-dihydro-oxazol-2-ylamine,
(RS)-4-(4-chloro-3-methyl-phenyl)-4-methyl-4,5-dihydro-oxazol-2-ylamine,
(RS)-4-(5-chloro-2-methyl-phenyl)-4,5-dihydro-oxazol-2-ylamine,
(RS)-4-(4-chloro-2-fluoro-5-methyl-phenyl)-4-methyl-4,5-dihydro-oxazol-2-ylamine,
(S)-4-(4-chloro-3-methyl-phenyl)-4-methyl-4,5-dihydro-oxazol-2-ylamine,
(RS)-4-(4-bromo-2-trifluoromethyl-phenyl)-4,5-dihydro-oxazol-2-ylamine,
(S)-4-(4-chloro-2-fluoro-5-methyl-phenyl)-4-methyl-4,5-dihydro-oxazol-2-ylamine,
(+)-(8)-4-(5-chloro-2-methyl-phenyl)-4,5-dihydro-oxazol-2-ylamine,
(RS)-4-(4-fluoro-2-methyl-phenyl)-4,5-dihydro-oxazol-2-ylamine,
(+)-(S)-4-(4-bromo-2-trifluoromethyl-phenyl)-4,5-dihydro-oxazol-2-ylamine,
(+)-(S)-4-(5-chloro-2-trifluoromethyl-phenyl)-4,5-dihydro-oxazol-2-ylamine,
(RS)-4-(4-chloro-2-ethyl-phenyl)-4,5-dihydro-oxazol-2-ylamine,
(+)-(S)-4-(4-fluoro-2-methyl-phenyl)-4,5-dihydro-oxazol-2-ylamine,
(RS)-4-(3-chloro-4-methyl-phenyl)-4,5-dihydro-oxazol-2-ylamine,
(RS)-4-(4-chloro-2-cyclopropyl-phenyl)-4,5-dihydro-oxazol-2-ylamine,
(S)-4-(4-chloro-2-ethyl-phenyl)-4,5-dihydro-oxazol-2-ylamine,
(RS)-4-(3-fluoro-2-methyl-phenyl)-4,5-dihydro-oxazol-2-ylamine,
(S)-4-(4-chloro-2-cyclopropyl-phenyl)-4,5-dihydro-oxazol-2-ylamine,
(RS)-4-(3-fluoro-2-trifluoromethyl-phenyl)-4,5-dihydro-oxazol-2-ylamine or
(S)-4-(3-chloro-4-methyl-phenyl)-4,5-dihydro-oxazol-2-ylamine,
(S)-4-[2-(4-fluoro-phenyl)-ethyl]-4,5-dihydro-oxazol-2-ylamine,
(S)-4-[2-(4-fluoro-3-methoxy-phenyl)-ethyl]-4,5-dihydro-oxazol-2-ylamine,
((S)-4-[2-(2,4-differenl)-ethyl]-4,5-dihydro-oxazol-2-ylamine,
(S)-4-[2-(3,4-debtor-phenyl)-ethyl]-4,5-dihydro-oxazol-2-ylamine,
(S)-4-[2-(2-trifluoromethyl-phenyl)-ethyl]-4,5-dihydro-oxazol-2-ylamine,
(S)-4-[2-(2-fluoro-phenyl)-ethyl]-4,5-dihydro-oxazol-2-ylamine,
(S)-4-[2-(3-fluoro-phenyl)-ethyl]-4,5-dihydro-oxazol-2-ylamine,
(S)-4-[2-(3,5-debtor-phenyl)-ethyl]-4,5-dihydro-oxazol-2-ylamine,
(S)-4-(2-ortho-tolyl-ethyl)-4,5-dihydro-oxazol-2-ylamine,
(S)-4-(2-meta-tolyl-ethyl)-4,5-dihydro-oxazol-2-ylamine,
(S)-4-(2-para-tolyl-ethyl)-4,5-dihydro-oxazol-2-ylamine,
(S)-4-[2-(4-trifluoromethyl-phenyl)-ethyl]-4,5-dihydro-oxazol-2-ylamine,
(S)-4-[2-(3-trifluoromethyl-phenyl)-ethyl]-4,5-dihydro-oxazol-2-ylamine,
(R)-4-[2-(3,4-dichloro-phenyl)-ethyl]-4,5-dihydro-oxazol-2-ylamine,
(S)-4-[2-(3,4-dichloro-phenyl)-ethyl]-4,5-dihydro-oxazol-2-ylamine,
(S)-4-[2-(4-chloro-2-fluoro-phenyl)-ethyl]-4,5-dihydro-oxazol-2-ylamine,
(S)-4-[2-(4-fluoro-3-trifluoromethyl-phenyl)-ethyl]-4,5-dihydro-oxazol-2-ylamine,
(S)-4-[2-(3-fluoro-4-trifluoromethyl-phenyl)-ethyl]-4,5-dihydro-oxazol-2-ylamine,
(S)-4-[2-(3,5-dichloro-phenyl)-ethyl]-4,5-dihydro-oxazol-2-ylamine,
(S)-4-[2-(2-chloro-4-fluoro-phenyl)-ethyl]-4,5-dihydro-oxazol-2-ylamine,
(S)-4-[2-(4-fluoro-3-methyl-phenyl)-ethyl]-4,5-dihydro-oxazol-2-ylamine,
(S)-4-{2-[3-(1,1,2,2-titrator-ethoxy)-phenyl]-ethyl}-4,5-dihydro-oxazol-2-ylamine,
(S)-4-[2-(2-fluoro-3-trifluoromethyl-phenyl)-ethyl]-4,5-dihydro-oxazol-2-ylamine,
(S)-4-[2-(3-bromo-phenyl)-ethyl]-4,5-dihydro-oxazol-2-ylamine,
(S)-4-[2-(4-chloro-3-trifluoromethyl-phenyl)-ethyl]-4,5-dihydro-oxazol-2-ylamine,
()-4-[2-(3-fluoro-4-triptoreline-phenyl)-ethyl]-4,5-dihydro-oxazol-2-ylamine,
(S)-4-[2-(4-fluoro-3-triptoreline-phenyl)-ethyl]-4,5-dihydro-oxazol-2-ylamine,
(S)-4-[2-(2,3-dichloro-phenyl)-ethyl]-4,5-dihydro-oxazol-2-ylamine,
(S)-4-[2-(3-chloro-4-triptoreline-phenyl)-ethyl]-4,5-dihydro-oxazol-2-ylamine,
(S)-4-[2-(2-chloro-3-trifluoromethyl-phenyl)-ethyl]-4,5-dihydro-oxazol-2-ylamine,
(S)-4-(1-methyl-2-phenyl-ethyl)-4,5-dihydro-oxazol-2-ylamine,
(S)-4-[2-(2-fluoro-5-trifluoromethyl-phenyl)-ethyl]-4,5-dihydro-oxazol-2-ylamine,
(S)-4-[2-(3-fluoro-5-trifluoromethyl-phenyl)-ethyl]-4,5-dihydro-oxazol-2-ylamine,
(S)-4-[2-(2,5-bis-trifluoromethyl-phenyl)-ethyl]-4,5-dihydro-oxazol-2-ylamine,
(S)-4-[2-(4-chloro-phenyl)-butyl]-4,5-dihydro-oxazol-2-ylamine,
(S)-4-(2-phenyl-butyl)-4,5-dihydro-oxazol-2-ylamine,
(S)-4-[2-(4-trifluoromethyl-phenyl)-propyl]-4,5-dihydro-oxazol-2-ylamine,
(S)-4-[2-(4-trifluoromethyl-phenyl)-butyl]-4,5-dihydro-oxazol-2-ylamine,
(S)-4-[2-(3-trifluoromethyl-phenyl)-propyl]-4,5-dihydro-oxazol-2-ylamine,
(S)-4-[2-(3-trifluoromethyl-phenyl)-butyl]-4,5-dihydro-oxazol-2-ylamine,
(S)-4-[2-(3,5-debtor-phenyl)-propyl]-4,5-dihydro-oxazol-2-ylamine,
(S)-4-[2-(3,5-debtor-phenyl)-butyl]-4,5-dihydro-oxazol-2-ylamine,
(S)-4-[2-(4-fluoro-phenyl)-butyl]-4,5-dihydro-oxazol-2-ylamine,
(S)-4-[2-(3,4-debtor-phenyl)-butyl]-4,5-dihydro-oxazol-2-ylamine,
(S)-4-[2-(2-fluoro-phenyl)-propyl]-4,5-dihydro-oxazol-2-ylamine,
(S)-4-[2-(3,4-dichloro-phenyl)-propyl]-4,5-dihydro-oxazol-2-ylamine,
(S)-4-[2-(3,4-dichloro-phenyl)-butyl]-4,5-dihydro-oxazol-2-ylamine,
(S)-4-[2-(2-fluoro-phenyl)-butyl]-4,5-is hydro-oxazol-2-ylamine,
(S)-4-[2-(2-chloro-phenyl)-ethyl]-4-methyl-4,5-dihydro-oxazol-2-ylamine,
(S)-4-[2-(3-chloro-phenyl)-ethyl]-4,5-dihydro-oxazol-2-ylamine,
(S)-4-[2-(4-chloro-phenyl)-ethyl]-4-methyl-4,5-dihydro-oxazol-2-ylamine,
(S)-4-[2-(3-chloro-phenyl)-ethyl]-4-methyl-4,5-dihydro-oxazol-2-ylamine,
(S)-4-[2-(4-fluoro-phenyl)-ethyl]-4-methyl-4,5-dihydro-oxazol-2-ylamine,
(S)-4-[2-(4-chloro-phenyl)-ethyl]-4,5-dihydro-oxazol-2-ylamine,
(S)-4-[2-(2-chloro-phenyl)-ethyl]-4,5-dihydro-oxazol-2-ylamine,
(S)-4-[2-(3-chloro-phenyl)-butyl]-4,5-dihydro-oxazol-2-ylamine,
(S)-4-((S)-2-phenyl-butyl)-4,5-dihydro-oxazol-2-ylamine,
(S)-4-((R)-2-phenyl-butyl)-4,5-dihydro-oxazol-2-ylamine,
(S)-4-[2-(2-chloro-6-fluoro-phenyl)-ethyl]-4,5-dihydro-oxazol-2-ylamine,
(S)-4-[2-(2,4-dichloro-phenyl)-ethyl]-4-methyl-4,5-dihydro-oxazol-2-ylamine,
(S)-4-[2-(2-bromo-phenyl)-ethyl]-4,5-dihydro-oxazol-2-ylamine,
(S)-4-[2-(2,5-dichloro-phenyl)-ethyl]-4,5-dihydro-oxazol-2-ylamine,
(S)-4-[2-(3-fluoro-phenyl)-butyl]-4,5-dihydro-oxazol-2-ylamine,
(S)-4-[2-(3-chloro-2-fluoro-phenyl)-butyl]-4,5-dihydro-oxazol-2-ylamine,
(S)-4-[2-(3-chloro-4-fluoro-phenyl)-butyl]-4,5-dihydro-oxazol-2-ylamine,
(S)-4-[2-(3-chloro-5-fluoro-phenyl)-butyl]-4,5-dihydro-oxazol-2-ylamine,
(S)-4-[2-(5-chloro-2-fluoro-phenyl)-butyl]-4,5-dihydro-oxazol-2-ylamine,
(S)-4-(3-phenyl-propyl)-4,5-dihydro-oxazol-2-ylamine,
(R)-4-(3-phenyl-propyl)-4,5-dihydro-oxazol-2-ylamine,
(R)-4-phenylsulfanyl-4,5-dihydro-oxazol-2-ylamine,
(R)-4-benzosulfimide-4,5-dihydro-oxazol-2-ylamine,
(R)-4-bansilal animetal-4,5-dihydro-oxazol-2-ylamine,
(R)-4-(4-chloro-phenylsulfonyl)-4,5-dihydro-oxazol-2-ylamine,
(S)-4-[1-(4-chloro-phenyl)-cyclopropylmethyl]-4,5-dihydro-oxazol-2-ylamine,
(S)-4-[1-(4-chloro-phenyl)-cyclobutylmethyl]-4,5-dihydro-oxazol-2-ylamine,
(S)-4-(1-phenyl-cyclopropylmethyl)-4,5-dihydro-oxazol-2-ylamine,
(R)-4-[(dimethyl-phenyl-silanol)-methyl]-4,5-dihydro-oxazol-2-ylamine,
(RS)-4-(2,3-dihydro-benzo[1,4]dioxin-6-yl)-4,5-dihydro-oxazol-2-ylamine,
(RS)-4-naphthalene-1-yl-4,5-dihydro-oxazol-2-ylamine,
(R)-4-naphthalene-1-ylmethyl-4,5-dihydro-oxazol-2-ylamine,
(S)-4-naphthalene-1-ylmethyl-4,5-dihydro-oxazol-2-ylamine,
(RS)-4-(1,2,3,4-tetrahydro-naphthalene-2-yl)-4,5-dihydro-oxazol-2-ylamine,
(S)-4-naphthalene-2-yl-4,5-dihydro-oxazol-2-ylamine,
(S)-4-[2-(3-fluoro-pyridine-4-yl)-ethyl]-4,5-dihydro-oxazol-2-ylamine,
(S)-4-[2-(6-trifluoromethyl-pyridin-2-yl)-ethyl]-4,5-dihydro-oxazol-2-ylamine,
(S)-4-[2-(2-methyl-pyridin-4-yl)-ethyl]-4,5-dihydro-oxazol-2-ylamine or
(S)-4-(2-cyclohexyl-ethyl)-4,5-dihydro-oxazol-2-ylamine
the effective amount and a pharmaceutically acceptable excipients.

44. The pharmaceutical composition according to item 43 for the treatment of anxiety disorders, bipolar disorder, attention deficit disorder and hyperactivity disorder, disorders caused by stress, psychotic disorders, schizophrenia, neurological diseases, Parkinson's disease, neurodegenerative disorders, Alzheimer's disease, epilepsy or migraine./p>

45. The pharmaceutical composition according to item 44, containing one or more than one compound according to item 44, for the treatment of psychosis, Parkinson's disease, anxiety, and attention deficit disorder and hyperactivity disorder (ADHD).



 

Same patents:

FIELD: chemistry.

SUBSTANCE: invention relates to novel disubstituted phenylpyrrolidines of formula , any stereoisomers thereof or any mixtures of stereoisomers thereof, or N-oxides thereof, or pharmaceutically acceptable salts thereof, where Ar denotes phenyl; R1 denotes F, Cl; R2 denotes F and Cl; R3 denotes H, Me, Et, n-Pr, iso-Pr, n-Bu, iso-Bu, sec-Bu, tert-Bu, cyclopropylmethyl, CFH2CH2CH2-, CF2HCH2CH2-, CF3CH2CH2-, allyl and CH3OCH2CH2-; X denotes F, OH; under the condition that X denotes OH, R3 does not denote H.

EFFECT: compounds are capable of increasing levels of dopamine, norepinephrine and serotonin, which enables their use in treating central nervous system disorders.

16 cl, 21 dwg, 69 ex

FIELD: chemistry.

SUBSTANCE: invention relates to indole derivatives or pharmaceutically acceptable salts thereof of general formula (1): , where values of R1, R2, m are given in claim 1.

EFFECT: compounds have inhibiting activity on IKKβ, which enables their use as a preventive or therapeutic agent for treating IKKβ mediated diseases.

26 cl, 1 tbl, 29 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention relates to pharmaceutical composition for treating diabetes, obesity or metabolic syndrome, which includes therapeutically efficient amount of (5-hydroxyadamantan-2-yl)amide of trans-2'-tret-butyl-2'H-[1,3']bipyrazolyl-4'-carboxylic acid or its pharmaceutically acceptable salts, and pharmaceutically acceptable carrier.

EFFECT: invention also relates to application of said compound for preparation of medication, intended for treatment of said diseases.

2 cl, 1 tbl, 99 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: present invention refers to 11-(piperazin-1-yl) dibenzo[b,f[1,4]oxazapine compounds of general formula specified below wherein the radicals are presented in the description, to their pharmaceutically acceptable salts and pharmaceutical compositions. There are also described methods for preparing said compounds.

EFFECT: compounds may be used for treating disorders, such as schizophrenia, resistant schizophrenia, bipolar disorder, psychotic depression, resistant depression, depressive conditions related to schizophrenia, treating resistant OCD, autism, senile dementia, psychotic dementia, L-DOPA-induced psychotic disorder, psychogenic polydipsia, psychotic symptoms of neurological disorders, sleeping disorders.

39 cl, 25 ex, 8 dwg

FIELD: medicine.

SUBSTANCE: invention relates to condensed bicyclic compounds, having affinity with mineralocorticoid receptor (VR) of formula [I] and formula [ii], as well as to pharmaceutical compositions on their basis. In general formula [I[ and [ii] ring A represents benzene ring, which has substituent R1, condensed with adjacent 6-membered heterocyclic ring, and said benzene ring additionally optionally is substituted with one or two substituent(s), selected from halogen atom and C1-8-alkyl group, R1 represents C1-8-alkylsulfonyl amino group or C1-8-alkyl aminosulfonyl group, R2 and R3 (a) are similar or different and represent group, selected from hydrogen atom, C1-8-alkyl group, and from 6- to 10-membered monocyclic or bicyclic aryl group (said aryl group is optionally substituted with halogen atom), (b) are combined with each other with formation of oxogroup or (c) are combined with each other on their ends together with adjacent carbon atom with formation of C3-10-cycloalkyl group, X represents the following group =N-, =C(R4)- or -CH(R4)-, R4 represents hydrogen atom, cyanogroup, halogen atom, C1-6-alkyl group, C2-6-alkenyl group, C3-10-dicloalkyl group, C1-7-alkanoyl group, carbamoyl group or C3-8cycloalkenyl group, Ar represents from 6- to 10-membered monocyclic or bicyclic aryl group, optionally containing one or several heteroatom(s), selected from sulphur atom, oxygen atom and nitrogen atom (said aryl group is optionally substituted with similar or different, one or two substituent(s), selected from halogen atom, cyanogroup, C1-8-alkyl group, trihalogen- C1-8-alkyl group and C1-8alkoxygroup), and dotted line represents presence or absence of double bond, Xa represents the following group =N- or =C(CN)-, RZ represents hydrogen atom or halogen atom, R25 and R35 represent alkyl group, and Ar3 represents phenyl group, optionally substituted with one or two group(s), which is(are) selected from halogen atom and trihalogenalkyl group.

EFFECT: compounds can be applied as antihypertensive medication.

15 cl, 18 tbl, 8 dwg, 71 ex

FIELD: chemistry.

SUBSTANCE: invention relates to novel derivatives of dihydroquinone and dihydronaphthyridinone of formula (I) or to its pharmaceutically acceptable salts, in which X represents group CR11 or N; Y represents group -C(O)R3, oxazolyl or isoxazolyl; Z represents phenyl, pyrrolidinyl, piperidinyl, morpholinyl, tetrahydropyranyl, pyridinyl, pyrimidinyl or pyrazolyl, and is substituted with groups R1 and R2; R1 and R2 each independently represents H, halogen, CN group, C1-6alkyl or group -Y1-Y2-Y3-R8, or R1 and R2 together form group -O(CH2)nO-, where n represents 1 or 2; Y1 represents group -O-, -C(O)-, -C(O)O-, -C(O)NR9-, -NR9C(O), -S-, -SO2- or bond; Y2 represents heterocycloalkylene, C1-6alkylene or bond, where heterocycloalkylene stands for cycloalkylene group, in which one, two carbon atoms are substituted with heteroatoms O or N, where heterocycloalkylene group also contains, at least, two carbon atoms and cycloalkylene represents ; Y3 represents group -O-, -C(O)-, -C(O)O-, -C(O)NR9-, -NR9C(O)-, -SO2- or bond; R8 represents H, C1-6alkyl, C1-6alkoxy, cyclohexyl, pyrrolidinyl, piperidinyl, morpholinyl, piperazinyl, tetrahydropyranyl, or group -NR9R10, where R8, different from H, is optionally substituted with C1-6alkyl, halogen, group -CF3 or group -OH; R9 and R10 each independently represents H or C1-6alkyl; R3 represents OH, C1-6alkyl, C1-6alkoxy, (C1-6alkoxy)-C1-6alkoxy; R4 represents C1-6alkyl, phenyl, cyclopropyl, cyclobutyl, cyclobutyl, cyclohexyl, tetrahydropyranyl or tetrahydrothiophene 1,1 -dioxide, and is optionally substituted with C1-6alkyl, hydroxyl group, C1-6alkoxy, halogen, nitro group, amino group, cyano group or halo-lower alkyl; R5 and R6 each independently represents H, halogen, C1-6alkyl, group -CF3, C1-6alkoxy; R7 represents H; R11 represents H. Invention also re4lates to pharmaceutical composition based on formula (I) compound.

EFFECT: obtained are novel dihydroquinone and dihydronaphthyridinone derivatives, useful for treatment of disease mediated by JNK kinase.

9 cl, 4 tbl, 38 ex

FIELD: chemistry.

SUBSTANCE: invention relates to compound of formula , where A, Q, R1, R2, R3, R4, R5' are represented in i.1 of the formula, as well as to its hydrates, solvates and pharmaceutically acceptable salts, Also described are application of said compound and pharmaceutical composition, including such compound, for treatment of disease condition in mammals, which is sensitive to action of antagonists of vasopressin V1a, V1b or V2 receptors.

EFFECT: increase efficiency of compound application.

20 cl, 13 ex, 1 dwg

FIELD: medicine.

SUBSTANCE: invention refers to a compound of formula (I), its optical isomer or pharmaceutically acceptable salt, R is specified in cl.1 of the patent claim. The compounds may be presented both as an optical isomer, and as a racemic substance, and may be used for mental disorders, such as schizophrenia.

EFFECT: higher efficacy of using the compounds.

8 cl, 4 tbl, 3 dwg, 7 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: present invention offers compounds presented by general formula (I): or their pharmaceutically acceptable salts wherein R1, R2, R3 and R4 are presented in the description and exhibit substantial COMT inhobotory activity. Besides, the present invention described pharmaceutical compositions inhibiting catechol-O-transferase activity which contain the compound or its pharmaceutically acceptable salt as an active ingredient, and a pharmaceutically acceptable carrier.

EFFECT: there are declared pharmaceutical combinations for treatment or prevention of Parkinson's disease which contain (1) the pharmaceutical composition containing the compound under any cl 1-8 or its pharmaceutically acceptable salt and the pharmaceutically acceptable carrier, and (2) at least one compound specified in L-dope or carbidole.

10 cl, 9 ex, 17 tbl

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to new compounds of formula (VI): or its pharmaceutically acceptable salts; wherein n is equal to 0, 1, 2 or 3; R1 means -OH, H; R2a means OH, -CH3, provided at least one of R1 and R2a means -OH;R3 means Cl, Br, cyclopropyl, branched C3-5alkyl R4a means H; R8 means H; wherein the fragment: may be one of the groups B8, B35, B36, B37, B38, B39, B40, B41, B42, B43, B45, B46, B48, B54, B56, B58, B59, B61, B62, B71, B72, B74, B75, B76, B77, B78, B79, B80, B81, B82, B84, B86, B87, B88, B89, B90, B91, B93, B94, B95, B96, B97, B98, B99, B100 and B101 wherein the values are disclosed in the patent claim 1.

EFFECT: compounds show Hsp90 inhibitory activity that enables using them for treating the diseases caused by abnormal cell growth in mammals.

26 cl, 8 dwg, 2 tbl, 82 ex

FIELD: chemistry.

SUBSTANCE: invention relates to novel derivatives of 2-heteroaryl-substituted benzothiophene and benzofuran, precursors thereof and therapeutic use of said compounds, having structural formula (1a) where R1, R2, X9 and Q assume values given in the description, and pharmaceutically acceptable salts thereof, which are suitable for imaging amyloid deposits in living patients. The invention also relates to pharmaceutical compositions based on compounds of formula 1a, use and methods of producing said compounds. More specifically, the present invention relates to a method of imaging brain amyloid deposits in vivo for intravital diagnosis of Alzheimer's disease, and measuring clinical efficiency of therapeutic agents against Alzheimer's disease.

EFFECT: high efficiency of using said compounds.

15 cl, 1 tbl, 14 ex

FIELD: chemistry.

SUBSTANCE: invention relates to novel disubstituted phenylpyrrolidines of formula , any stereoisomers thereof or any mixtures of stereoisomers thereof, or N-oxides thereof, or pharmaceutically acceptable salts thereof, where Ar denotes phenyl; R1 denotes F, Cl; R2 denotes F and Cl; R3 denotes H, Me, Et, n-Pr, iso-Pr, n-Bu, iso-Bu, sec-Bu, tert-Bu, cyclopropylmethyl, CFH2CH2CH2-, CF2HCH2CH2-, CF3CH2CH2-, allyl and CH3OCH2CH2-; X denotes F, OH; under the condition that X denotes OH, R3 does not denote H.

EFFECT: compounds are capable of increasing levels of dopamine, norepinephrine and serotonin, which enables their use in treating central nervous system disorders.

16 cl, 21 dwg, 69 ex

FIELD: chemistry.

SUBSTANCE: invention relates to a method of producing 3-alkyl(aryl)-2,2'-bithiophene-5-carboxylic acids and esters thereof of general formula I where R = C1-C10-alkyl or aryl; R1 = hydrogen atom or C1-C4 alkyl, involving reaction of 2-acyl thiophenes of general formula II with dimethyl formamide and phosphoryl chloride, and the formed 2-alkyl(aryl)-3-chloro-3-(2-thienyl)acrylaldehyde of general formula III reacts with thioglycolic ester in the presence of a base, and by hydrolysis of the obtained esters of general formula I, where R assumes values given above and R1=C1-C4 alkyl, 3-alkyl-2,2'-bithiophene-5-carboxylic acids are obtained, where R1 = hydrogen atom.

EFFECT: simpler method of producing compounds of formula I, which can be used in synthesis of solvatochromic and thermochromic dendrimers, oligothiophenes with adjustable electrical and optical properties.

1 cl, 4 ex

FIELD: chemistry.

SUBSTANCE: invention relates to indole derivatives or pharmaceutically acceptable salts thereof of general formula (1): , where values of R1, R2, m are given in claim 1.

EFFECT: compounds have inhibiting activity on IKKβ, which enables their use as a preventive or therapeutic agent for treating IKKβ mediated diseases.

26 cl, 1 tbl, 29 ex

FIELD: chemistry.

SUBSTANCE: invention relates to a method of producing 2,3-disubstituted indoles of general formula (I): , where the method involves the following steps: a) reaction of bromine diol (i): with dialkoxyborane in the presence of a ligand, a palladium catalyst, preferably selected from Pd(OAc)2, PdCl2, PdBr2, Pd2(dba)3, Pd2(dba)3.CHCl3, [Pd(ally)Cl]2,- Pd(CH3CN)2Cl2, Pd(PhCN)2Cl2, Pd/C and encapsulated Pd and a base to obtain a compound of general formula or, alternatively, reaction of compound (i) with a magnesium compound containing 3 alkyl groups, with subsequent treatment with a borate to obtain a compound of general formula ii given above; b) reaction of the product from step (a) with R2-Hal to obtain a compound of general formula I; where: R denotes (C1-C6)alkyl; R2 denotes: , , , , ,

, , , , ;

R3 denotes cyclopentyl: X denotes carboxymethyl; Hal denotes Br or I; or pharmaceutically acceptable salt thereof.

EFFECT: higher efficiency.

12 cl, 4 dwg, 2 tbl, 14 ex

FIELD: chemistry.

SUBSTANCE: described are novel 1,2,4-triazolones of general formula (I):

, where A denotes N and values of other radicals are given in the claim, which are vasopressin receptor inhibitors, synthesis method thereof and use thereof to prepare medicinal agents for treating and/or preventing diseases, particularly for treating and/or preventing cardiovascular diseases.

EFFECT: high efficiency of using said derivatives.

6 cl, 512 ex

FIELD: chemistry.

SUBSTANCE: invention relates to novel pyrimidine derivatives of formula (1) in free form or in form of a salt. In formula (1): X1 and X2 all independently denote halogen; A denotes a radical of formula where (R1)1-2 denotes 1-2 identical or different substitutes selected from a group comprising C1-C4-alkyl, halogen-C1-C4-alkyl, hydroxy-C1-C4-alkyl, C1-C4-alkoxy-C1-C4-alkyl, R2R3N-C1-C4-alkyl, halogen, hydroxy group, C1-C4-alkoxy group, halogen-C1-C4-alkoxy group, C1-C4-alkylthio group, C1-C4-alkanoyl, C1-C4-alkanoylamino group, C1-C4-alkylsulphonylamino group, C1-C4-alkylsulphonyl, C1-C4-alkylthionyl, NR2R3 and morpholinyl; or A denotes a radical of formula where ring (a) denotes a 5-member heterocyclic ring containing 1 or 2 heteroatoms selected from a group comprising O and N, which can further be substituted with C1-C4-alkyl, and which is annelated in positions 3 and 4; and R2 and R3 all independently denote hydrogen or C1-C4-alkyl. The invention also relates to a parasite control composition containing said compounds, a parasite control method on warm-blooded animals and use of compounds of formula (1) to prepare a parasite control composition.

EFFECT: high efficiency of using said compounds.

11 cl, 7 ex, 2 tbl

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to a new compound of formula A

the radicals R1, R2, R3, R4, R5, R25, R26, U, T, W, V, Y are those as specified in clause 1 of the patent claim. Also, the invention refers to a method for preparing the compound of formula A, the drug based on this compound applied for treating disorders or diseases which are at least partially mediated by vanilloid receptor VR1 /NRPV1, as well as use of this compound for preparing the drug.

EFFECT: there are prepared and described new compounds which can be effective in treating diseases which are at least partially mediated by vanilloid receptor VR1 /NRPV1.

43 cl, 367 ex, 4 tbl

FIELD: chemistry.

SUBSTANCE: invention relates to novel substituted methyl-amines of general formula 1, having serotonin 5-HT6 receptor antagonist properties. In formula 1 , W is naphthalene, indolysin or quinoline; R1 is hydrogen, fluorine, chlorine, methyl; R2 is hydrogen, fluorine, methyl, phenyl, thiophen-2-yl, furan-2-yl, pyridyl, piperazin-1-yl or 4-methylpiperazin-1-yl; R3 is methyl; or W is benzene, R3 assumes the value given above; R1 is 3-Cl, R2 is 3-piperazin-1-yl or 3-(4-methylpiperazin-1-yl); or R1 is hydrogen, R2 is phenyl or pyridyl; or R1 is hydrogen, fluorine, chlorine, methyl; R2 is 4-piperazin-1-yl or 4-(4-methylpiperazin-1-yl); or W is oxazole, R3 is optionally substituted methyl; R1 is chlorine or fluorine, R2 is methyl, or R1 is hydrogen, fluorine, chlorine, methyl; R2 is piperazin-1-yl, 4-methylpiperazin-1-yl, or R1 is chlorine, fluorine or methyl; R2 is furan-2-yl, or R1 is hydrogen, fluorine, chlorine, methyl; R2 is furan-2-yl, R3 is (tetrahydrofuran-2-yl)methyl, or R1 is hydrogen, fluorine, chlorine, methyl; R2 is thiophen-2-yl, R3 is 2-methoxyethyl, or R1 is chlorine or fluorine, R2 is thiophen-2-yl, R3 is methyl.

EFFECT: compounds can be used to treat central nervous system (CNS) diseases, such as psychiatric disorders, schizophrenia, anxiety disorders, as well as for improving mental capacity, for treating obesity or for studying the molecular mechanism of inhibiting serotonin 5-HT6 receptors.

15 cl, 27 dwg, 2 tbl, 25 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: claimed invention relates to novel antibacterial chinolin derivatives of formula (1a), their stereochemically isomeric forms, N-oxides and pharmaceutically acceptable salts and solvates , where p equals 1; q equals 0, 1, 2, 3 or 4; R1 represents hydrogen, halogen, aryl or Het; R2 represents hydrogen or alkyloxy; R3 represents arylalkyl; each R4 and R5 independently represent hydrogen or alkyl; R7 represents hydrogen, alkyl or aryl; where aryl is selected from phenyl or naphtyl and is optionally substituted with 1, 2 or 3 substituents selected from hydroxy, halogen, cyano, nitro, amino, mono- or dialkylamino, alkyl, C2-6alkenyl, optionally substituted with phenyl, halogenalkyl, alkyloxy, halogenalkyloxy, carboxyl, alkyloxycarbonyl, aminocarbonyl, morpholinyl or mono- or dialkylaminocarbonyl; where Het is selected from furanyl, thienyl, pyridinyl, benzofuranyl, optionally substituted with 1, 2 or 3 substituents selected from halogen, hydroxyl, alkyl or alkyloxy.

EFFECT: compounds can be used for creation of preparations on their base for treatment of bacterial infection

21 cl, 4 ex, 3 tbl

FIELD: chemistry.

SUBSTANCE: invention is a 6-10-member aryl selected from phenyl, naphthyl, tetrahydronaphthalenyl, indanyl or a 6-member heteroaryl containing 1-2 N atoms, selected from pyridyl or pyrimidinyl, where the aryl and heteroaryl groups can be unsubstituted or substituted with 1-3 substitutes selected from a group consisting of C3-6-cycloalkyl, phenyl, phenyloxy, benzyl, benzyloxy, halogen atom, C1-7-alkyl, C1-7-alkoxy, oxazolyl, piperidin-1-yl, or C1-7-alkyl, substituted with a halogen atom, or represents phenyl, where at least one hydrogen atom is substituted with deuterium or tritium; R2 is a hydrogen atom, C1-7-alkyl or is benzyl, unsubstituted or substituted C1-7-alkoxy or halogen atom; or R1 and R2 together with a N atom with which they are bonded form 2,3-dihydroindol-1-yl or 3,4-dihydro-1quinolin-1-yl. The invention also relates to a method of producing compounds of formula and to a pharmaceutical composition having high affinity for the TAAR1 receptor.

EFFECT: compounds of formula (I), having high affinity for the TAAR1 receptor.

29 cl, 4 dwg, 1 tbl, 183 ex

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