INDOLES USEFUL IN TREATMENT ANDROGEN RECEPTORS BOUND DESEASES Russian patent published in 2008 - IPC C07D209/30 C07D401/06 C07D401/12 C07D413/06 A61K31/404 A61P5/24 

Abstract RU 2328484 C2

FIELD: chemistry.

SUBSTANCE: invention relates to the novel indole derivatives with the formula , where X means S, SO, SO2; R1 means 6-membered mono-homocyclic saturated or unsaturated ring structure or 5-, 6-membered monohetercyclic saturated or unsaturated ring structure with one or two heteratoms, chosen from N, O, S, and each of the said structures is not necessarily substituted with one or more substituters, chosen from the group, consisting of halogen, CN, (1C-4C)fluoroalkyl, NO2, (1C-4C)alkyl, (1C-4C)alkoxi or (1C-4C)fluoroalkoxi; R2 means 2-nitorphenyl, 2-cyanophenyl, 2-hydroxymethylphenyl, pyridine-2-il, pyridine-2-il-N-oxide, 2-benzamide, methylic ether of the 2-benzoic acid or 2-methoxyphenyl; R3 means H, halogen or (1C-4C)alkyl; R4 means H, OH, (1C-4C) alkoxy or halogen; R5 means H, OH, (1C-4C) alkoxy, NH2 CN, halogen, (1C-4C)fluoroalkyl, NO2, hydroxy(1C-4C)alkyl, CO2H, CO2(1C-6C)alkyl, or R5 means NHR6, where R6 means (1C-6C)acyl, not necessarily substituted with one or more halogens, S(O)2(1C-4C)alkyl or S(O)2heteroaryl, not necessarily substituted with (1C-4C)alkyl or one or more halogens, where heteroaryl is the 5-membered mono-heterocyclic unsaturated ring structure with one S atom or two N atoms, or R5 means C(O)N(R8,R9), where R8 and R9 , each independently, mean H, (3C-6C)cycloalkyl or CH2R10, where R10 means H, (1C-5C)alkyl, hydroxy(1C-3C)alkyl, complex (1C-4C)alkyl ether of the carboxy(1C-4C)alkyl, (1C-3C)alkoxy(1C-3C)alkyl, (mono- or di(1C-4C)alkyl)aminomethyl, (mono- or di1C-4C)alkyl)aminocarbonyl or pyhenyl, where R8 and R9 together with N form 5- or 6-membered saturated aor unsaturated heterocyclic ring, not necessarily containing N or O as the second heteroatom, not necessarily substituted with (1C-4C)alkyl; or its saline or hydrated form.

EFFECT: allows using indoles for producing pharmaceutical agent and in method for inhibiting 5α-dihydrosterone activity.

17 cl, 7 dwg, 5 tbl, 25 ex

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RU 2 328 484 C2

Authors

Khermkens Pedro Kharol'D Khan

Stok Kherman Tejs

Terkhejs Nel'T'E Miranda

Lommerse Jokhannes Petrus Marija

Van Der Lou Jap

Dates

2008-07-10Published

2003-11-03Filed