Novel applications of porphyrin compounds

FIELD: medicine.

SUBSTANCE: invention relates to application of compound of formula I or II given below in preparation of medication for elimination or attenuation of microorganisms' growth in the way which includes subjection of said compound to exposure to source of light of photodynamic therapy or source of ultrasound of ultrasonic (sonodynamic) therapy, where X1, X2, X3 and X4 independently represent hydrogen atom, lipophylic part of molecule, phenyl group, lower alkyl, alkaryl or aralkyl group or cationic group of the following formula: -L-R1-N+(R2)(R3)R4 where: L represents binding (linking) part of molecule or is absent; R1 represents lower alkylene, lower alkenylene or lower alkinylene, which is optionally substituted with one or several substituents selected from lower alkyl, lower alkylene (optionally interrupted with oxygen), fluorine, OR5, C(O)R6, C(O)OR7, C(O)NR8R9, NR10R11 and N+R12R13R14; and R2, R3 and R4 independently represent H, aryl, lower alkyl, lower alkenyl or lower alkinyl, three latter of which are optionally substituted with one or several substituents selected from lower alkyl, lower alkylene (optionally interrupted with oxygen), aryl, OR5, C(O)R6, C(O)OR7, C(O)NR8R9, NR10R11 and N+R12R13R14; Z represents -CH or N; Y1, Y2, Y3 and Y4 are absent or independently represent aryl, lower alkyl, lower alkenyl or lower alkinyl, three latter of which are optionally substituted with one or several substituents selected from lower alkyl, lower alkylene (optionally interrupted with oxygen), aryl, OR5, C(O)R6, C(O)OR7, C(O)NR8R9, NR10R11 and N+R12R13R14, or, taken together with pyrrolic ring, to which they are bound, can form cyclic group; and R5, R6, R7, R8, R9, R10, R11, R12, R13 and R14 independently represent H or lower alkyl; M represents element of metal or metalloid; on condition that at least one of X1, X2, X3 and X4 is cationic group, defined above, and at least one of X1, X2, X3 and X4 represents hydrogen atom, phenyl group, lipophylic part of molecule or lower alkyl, alkaryl or aralkyl group, said microorganisms being selected from bacteria, mycoplasms, yeasts and/or fungi. Invention also relates to method of treating patient who needs treatment with antimicrobial agent and method of eliminating microorganisms in vitro, including contact of said microorganisms with compound of formula

and

EFFECT: novel application of porphyrin compounds as antimicrobial agent, said microorganisms being selected from bacteria, mycoplasms, yeasts or fungi.

67 cl, 13 dwg, 4 tbl, 7 ex

 

The text descriptions are given in facsimile form.

1. The use of the compounds of formula I or II below, in the preparation of medicines for destruction or attenuate growth of microorganisms in a way that does not include the exposure of this compound to the action of the light source photodynamic therapy or source of ultrasound ultrasound (continuiously) therapy,

where X1, X2, X3and X4independently denote an atom bodoro is a, the lipophilic portion of the molecule, phenyl group, lower alkyl, albarillo or aracelio group or cationic group of the following formula
-L-R1-N+(R2)(R3R4,
where L denotes a linking (linker) the portion of the molecule or missing;
R1indicates the lowest alkylene, lower albaniles or lower akinyan, which is optionally substituted by one or more substituents selected from lower alkyl, lower alkylene (optionally interrupted by oxygen, fluorine, OR5C(O)R6C(O)OR7C(O)NR8R9, NR10R11and N+R12R13R14;
R2, R3and R4independently represent H, aryl, lower alkyl, lower alkenyl or lower quinil, the last three of which are optionally substituted by one or more substituents selected from lower alkyl, lower alkylene (optionally interrupted by oxygen), aryl, OR5C(O)R6C(O)OR7C(O)NR8R9, NR10R11and N+R12R13R14;
Z represents CH or N;
Y1, Y2, Y3and Y4absent or independently represent aryl, lower alkyl, lower alkenyl or lower quinil, the last three of which are optionally substituted by one or more substituents selected from lower alkyl, lower alkylene(optionally interrupted by oxygen), aryl, OR5C(O)R6C(O)OR7C(O)NR8R9, NR10R11and N+R12R13R14or, taken together with the pyrrole ring to which they are attached, may form a cyclic group; and
R5, R6, R7, R8, R9, R10, R11, R12, R13and R14independently represent H or lower alkyl;
M represents a metal element or metalloid;
provided that at least one of X1, X2, X3and X4is a cationic group, as defined above, and at least one of X1, X2, X3and X4denotes a hydrogen atom, phenyl group, the lipophilic portion of the molecule or lower alkyl, albarillo or aracelio group, with the
these microorganisms are selected from bacteria, Mycoplasma, yeast and/or fungi.

2. The use according to claim 1, where the drug is intended for destruction or attenuate growth of microorganisms in a way that does not include the exposure of this compound to the action of a stimulus that activates antimicrobial activity.

3. The use according to claim 2, where this compound exhibits antimicrobial activity in the absence of irradiation light source for photodynamic therapy or ultrasound source.

4. The use according to any one of claims 1 to 3, where M train is achet bivalent or trivalent metallic element.

5. The use according to claim 4, where M is selected from Zn(II), Cu(II), La(III), Lu(III), Y(III), In(III), Cd(II), Mg(II), Al(III), Ru, Ni(II), Mn(III), Fe(III) and Pd(II).

6. The use according to any one of claims 1 to 3, where M denotes metallogeny element, such as silicon (Si) or germanium (Ge).

7. The use according to any one of claims 1 to 3, where Y1, Y2, Y3and Y4no.

8. The use according to any one of claims 1 to 3, where Z denotes-CH.

9. The use according to any one of claims 1 to 3, where R1denotes unsubstituted lower alkylenes, lower alkynylamino or lower alkynylamino group.

10. The use according to claim 9, where R1represents -(CH2)mand m is an integer of 1-20.

11. The use of claim 10, where 'm' is an integer from 1-10, for example, 1-6, 1-5, 1-4, or 1-3.

12. The application of claim 11, where m is equal to 3.

13. The use according to any one of claims 1 to 3, where R2, R3and/or R4denote lower alkyl, lower alkenylphenol or lower alkylamino group.

14. Use item 13, where R2, R3and/or R4denote unsubstituted lower alkyl groups.

15. Use item 13, where at least one of R2, R3and R4denotes an alkyl group that is substituted primary, secondary or tertiary amino group or Quaternary ammonium group.

16. The use according to any one of claims 1 to 3, where R1represents -(CH2)3-, R2and R3denote SN and R4represents -(CH2)3-N(CH3)2.

17. The use according to any one of claims 1 to 3, where R1represents -(CH2)3and R2, R3and R4denote each CH3.

18. The use according to any one of claims 1 to 3, where R1represents -(CH2)3and R2, R3and R4denote each With2H5.

19. The use according to claim 1, where L is selected from the group consisting of a linking group phenoxy, phenylene, sulfanilamide, aminosulfonyl, sulfonylamino, phenylcarbonylamino, phenylenesulfonyl, urea, urethane or carbamate.

20. The application of claim 19, where X1, X2, X3and/or X4denote

where R denotes the R1-N+(R2)(R3R4as defined in claim 1, and n is an integer of 1-3.

21. The application of claim 19, where X1, X2, X3and/or X4denote

where R denotes the R1-N+(R2)(R3R4as defined in claim 1, and m is an integer 1-3.

22. The application of claim 19, where X1, X2, X3and/or X4denote

where each R independently denotes an R1-N+(R2)(R3R4as defined in claim 1, and n and m are equal integers of 1-3, and where the sum n+m is an integer 1-3.

23. Application is on any of PP-22, where n or m is equal to 3.

24. The use according to any one of p-22, where n or m is 2.

25. The use according to any one of p-22, where n and/or m is 1.

26. The use according to any one of p-22, where L is monosubstituted in paraprotein.

27. The use according to any one of p-22, where L is monosubstituted or disubstituted in metabologia (metabolite).

28. The use according to any one of p-22, where L is monosubstituted or disubstituted in anthopology (ortobalagang).

29. The use according to any one of claims 1 to 3, where this compound contains two cationic groups, as defined in claim 1, on opposite sides of the porphyrin ring, i.e. in terms of ring 5 and 15 or the provisions of the rings 10 and 20.

30. The application of clause 29, where X1and X3are a hydrogen atom, a lipophilic group, phenyl group, lower alkyl, alkalline or aranceles group, and X2and X4are cationic groups or vice versa.

31. The use according to any one of claims 1 to 3, where this compound may contain two cationic groups, as defined in claim 1, adjacent the provisions of the porphyrin ring, i.e. in terms of ring 5 and 10, or the provisions of the ring 10 and 15, or the provisions of the ring 15 and 20, or the provisions of the rings 20 and 5.

32. Use p, where X1and X2represent hydrogen, and X3and X4denote a cationic group, or X2and X3oznachaet hydrogen, and X4and X1denote a cationic group.

33. The use according to any one of claims 1 to 3, where at least one of X1, X2, X3and X4denotes a lipophilic portion of the molecule.

34. Use p, where the lipophilic portion of the molecule is a saturated alkyl group branched chain of the formula -(CH2)PCH3where p is the number 1-22.

35. The application 34, where p is 1 to 18, for example 2-16 or 4-12.

36. The use according to any one of claims 1 to 3, where none of X1, X2, X3and X4is not lipophilic part of the molecule.

37. The use according to any one of claims 1 to 3, where none of X1, X2, X3and X4not a phenyl group.

38. The use according to any one of claims 1 to 3, where this compound is water soluble.

39. The use according to claim 1, where this connection is dichloride 5,15-bis-(4-{3-[(3-dimethylaminopropyl)dimethylammonio]propyloxy}phenyl)porphyrin.

40. The use according to claim 1, where this connection is dichloride 5,15-bis-[4-(3-triethylammonium)phenyl]porphyrin.

41. The use according to claim 1, where this connection is dichloride 5,15-bis-[3-(3-trimethylammoniumphenyl)phenyl]porphyrin.

42. The use according to claim 1, where this connection is dichloride 5,15-bis-[4-(3-trimethylammoniumphenyl)phenyl]porphyrin.

43. The use according to claim 1, where this connection is receiving dichloride is 5-[3,5-bis-(3-trimethylammoniumphenyl)phenyl]-15-undeciphered.

44. The use according to claim 1, where this connection is the chloride of 5-{4-[3-dimethyl-(3-dimethylaminopropyl)ammoniumnitrate]phenyl}-15-(4-dodecyloxyphenyl)porphyrin.

45. The use according to claim 1, where this connection is trichloride 3-[({3-[(3-{4-[15-4-dodecyl of oxyphenyl)
porphyrin-5-yl]phenoxy}propyl)dimethylammonio]propyl}-dimethylammonio)propyl]trimethylammonium.

46. The use according to claim 1, where this connection is dichloride 5,15-bis-[3-(3-trimethylammoniumphenyl)phenyl]-10-undeciphered.

47. The use according to claim 1, where this connection is dichloride, 5-{4-[3-dimethyl-(3-trimethylammonio)ammoniumnitrate]phenyl}-15-(4-dodecyloxyphenyl)porphyrin.

48. The use according to claim 1, where this connection is dichloride, 5-[4-(3-dimethylcyclopropane)phenyl]-15-{4-[3-dimethyl-(3-dimethylaminopropyl)ammoniumnitrate]phenyl}porphyrin.

49. The use according to any one of p-48, where this connection is metallizovannoj form.

50. The use according to any one of claims 1 to 3, where this compound is essentially non-toxic against mammalian cells.

51. The use according to any one of claims 1 to 3, where the drug is intended for oral administration.

52. The use according to any one of claims 1 to 3, where the drug is intended for parenteral administration.

53. The use according to any one of claims 1 to 3, where this drug environments is the primary objective is for local (topical) administration.

54. The use according to any one of claims 1 to 3, where these microorganisms are bacteria that are resistant to one or more conventional antibiotic agents.

55. The use according to any one of claims 1 to 3, where these microorganisms are not available for surface light or not available to light the area.

56. The use according to any one of claims 1 to 3, where the drug is intended for use in the treatment and/or prevention of microbial infections.

57. Use p, where the microbial infection is a systemic infection.

58. The use according to any one of claims 1 to 3, where the drug is intended for preventing and/or treating dermatological infections.

59. The use according to any one of claims 1 to 3, where the drug is intended for the prevention and/or treatment of infections of the lungs.

60. The use according to any one of claims 1 to 3, where the drug is intended for the prevention and/or treatment of wound infection and/or ulceration.

61. A method of treating a patient in need of treatment, an antimicrobial agent, providing for the introduction of this patient compounds described in any one of claims 1 to 50, where this method does not include the irradiation of this compound stimulus that activates antimicrobial activity, and these microorganisms are selected from bacteria, Mikaela is m, yeast and/or fungi.

62. The method according to p, where this compound is administered orally.

63. The method according to p, where this compound is administered parenterally.

64. The method according to p, where this compound is administered topically (topicaine).

65. The method according to p where this patient has a dermatological infection or infection of the lung.

66. The method according to p where this patient has a wound infection.

67. The method of killing microorganisms in vitro, providing for the participation of these microorganisms with the compound described in any one of claims 1 to 50, where this method does not include the exposure of this compound to the action of a stimulus that activates antimicrobial activity and
these microorganisms are selected from bacteria, Mycoplasma, yeast and/or fungi.



 

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15 cl, 4 dwg, 8 ex

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2 ex

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2 cl, 3 tbl, 9 ex

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21 cl, 64 ex

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40 cl, 14 ex

Antiviral agent // 2381807

FIELD: medicine.

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3 cl

FIELD: veterinary science.

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EFFECT: preparation and method exhibit high therapeutic efficiency in comparison with analogues.

4 cl, 4 tbl, 4 ex

FIELD: chemistry.

SUBSTANCE: invention relates to novel compounds of formula I with anti-HIV activity , where R1 represents C1-6(Ar1)alkyl or C1-6(Ar1)oxyalkyl; R2 represents hydrogen or OR14; R3 represents hydrogen, halogen, hydroxyl, cyano, C1-6alkyl, C5-7cycloalkenyl, C1-6halogenalkyl, C1-6alkoxy, C1-6alkylthio, N(R8)(R9), NHAr2, N(R6)COR7, OCON(R8)(R9), OCH2CON(R9)(R9), CO2R6, CON(R8)(R9), SOR7, S(=N)R7, SO2R7, SO2N(R6)(R6), PO(OR6)2, C2-4(R12)alkynyl, R13, Ar2 or Ar3; R4 represents hydrogen, halogen, C1-6alkyl or C1-6alkoxy; R5 represents hydrogen, halogen, C1-6alkyl or C1-6alkoxy; R6 represents hydrogen or C1-6alkyl; R7 represents C1-7alkyl; R8 represents hydrogen or C1-6alkyl; R9 represents hydrogen, C1-6alkyl, C1-6hydroxyalkyl or C1-6(C1-6dialkylamino)alkyl; or N(R8)(R9) taken together represent azetidinyl, pyrrolydinyl, (R10)-piperidinyl, N-(R11)-piperazinyl, morpholinyl or dioxothiazinyl; R10 represents hydrogen; R11 represents hydrogen, C1-6alkyl, COR6 or CO2R6 ; R12 represents hydrogen, hydroxyl, N(R6)(R6), OSO2R7 or dioxothiazinyl; R13 represents dioxothiazinyl; R4 represents hydrogen or C1-6alkyl; Ar1 represents ,,,,,,,,; or Ar2 represents tetrazolyl, triazolyl, thiadiazolyl, pyrazolyl, imidazolyl, oxazolyl, thiazolyl, isoxazolyl, furanyl, thienyl, pyrrolyl, pyrimidinyl, pyrazinyl, pyridinyl, quinolinyl or indolyl, and is substituted with 0-2 substitutes selected from a group consisting of halogen, benzyl, C1-6alkyl, C1-6alkoxy, N((R8)(R9), CON(R8)(R9) and CO2R8; Ar3 represents phenyl substituted with 0-2 substitutes selected from a group consisting of halogen, cyano, hydroxy, C1-6alkyl, C1-6alkoxy, (C1-6alkoxy)methyl, C1-6halogenalkoxy, N(R8)(R9), CON(R6)(R6) and CH2N(R8)(R9), or represents dioxolanylphenyl; and X-Y-Z represents C(R14)2OC(R14)2C(R14)2, C(R14)2OC(R14)2C(R14)2C(R14)2; or pharmaceutically acceptable salt thereof. The invention also relates to a pharmaceutical composition.

EFFECT: bicyclic heterocycles are disclosed, as well as their use HIV integrase inhibitors.

21 cl, 38 dwg, 8 tbl, 282 ex

FIELD: chemistry.

SUBSTANCE: present invention relates to piperidine-amino-benzidazoles having formula (I) and to addition salts or stereochemically isomeric forms, where Q is C1-6alkyl optionally substituted with one or two substitutes, each independently selected from a group consisting of trifluoromethyl, C3-7cycloalkyl, Ar2, hydroxyl, Ar2 - oxy-, hydroxycarbonyl, aminocarbonyl, C1-4alkylcarbonyl, aminocarbonyloxy, C1-4alkoxycarbonyl, Ar2(CH2)ncarbonyloxy, C1-4alkoxycarbonyl-(CH2)noxy, mono- or di(C1-4alkyl)aminocarbonyl, aminosulfonyl, mono(C1-4alkyl)aminosulfonyl, or heterocycle selected from a group consisting of pyrrolidinyl, dihydropyrrolyl, imidazolyl, triazolyl, homopiperidinyl, pyridyl and tetrahydropyridyl; or where Q is C1-6alkyl substituted with two substitutes, where substitute is an amino group and the other is C1-6alkyloxycarbonyl; G is -CH2-; R1 is pyridyl optionally substituted with two substitutes selected from a group consisting of hydroxyl, C1-6alkyl; each n equals 1; one of R2a and R3a is C1-6alkyl and the other is hydrogen; when R2a is not hydrogen, R2b is C1-6alkyl and R3b is alkyl; and R3a, R2a, R2b all represent hydrogen; or R5 is hydrogen; t equals 2; Ar2 is phenyl or phenyl substituted with one or more, for example 2 substitutes selected from halogen, C1-6alkyloxy, aminosulfonyl and C1-4alkoxycarbonyl. The invention also relates to a pharmaceutical composition based on compound of formula I and use of the said compounds in making medicinal agents.

EFFECT: novel piperadine-amino-benzimidazoles are obtained, having inhibitory effect on respiratory syncytial virus replication.

10 cl, 3 tbl, 5 ex

FIELD: medicine.

SUBSTANCE: invention relates to medicine, oncology, and can be used for treating basaliomas. For this purpose dissection of affected skin portions is performed including healthy tissues within 0.5 cm by means of surgical laser with wavelength 810 nm pulse duration 0.2-0.5 seconds radiating power 15 W. After that 0.1% Radachlorin gel is applied on affected surface in terms 0.2 g per 1 cm2 of surface. 2-hour exposition under light-tight bandage. After gel removal surface is processed by laser light with wavelength 662 nm with light energy dose 200 J/cm2. Exposure is performed without contact. As laser radiation source, diode laser apparatus for photodynamic therapy "LAHTA-MILON" can be used.

EFFECT: method allows to prevent cosmetic defect, post-operation complications due to quick healing of affected area, stop of tumor growth of tissues, reduces method traumatism and number of recurrences.

2 cl, 2 ex

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