公开(公告)号：RU2163808C2

公开(公告)日：2001-03-10

申请号：RU96121628

申请日：1995-03-23

Applicant: BASF AG

Inventor： EHRNST BAUMANN ,  UVE JOZEF FOGEL BAKHER ,  JOAKHIM RAJNKHAJMER ,  DAGMAR KLINGE ,  KHARTMUT RIKHERS ,  BURKKHARD KREGER ,  ZIGFRID BIALOJAN ,  KLAUS BOLL SHVAJLER ,  VOL FGANG VERNET ,  LILIANE UNGER ,  MANFRED RASHAK

IPC: A61K31/00 ,  A61K31/505 ,  A61K31/506 ,  C07D251/26 ,  A61K31/53 ,  A61P9/00 ,  A61P9/08 ,  A61P9/10 ,  A61P9/12 ,  A61P11/08 ,  A61P13/02 ,  A61P15/00 ,  A61P25/04 ,  A61P39/02 ,  C07D239/26 ,  C07D239/34 ,  C07D239/38 ,  C07D401/12 ,  C07D405/12 ,  C07D409/12 ,  C07D413/12 ,  C07D417/12

Abstract: organic chemistry, pharmacy. SUBSTANCE: invention proposes a novel drug showing inhibitory properties with respect to endothelin receptors. Invention proposes derivatives of carboxylic acid of the general formula (I): where R means formyl group, carboxyl group or residue easily hydrolyzed to carboxyl group; R2 and R3 means alkoxyl with carbon atoms number from 1 to 4; X means nitrogen atom or the group CH; R4,R5 and R6 means as given in the invention claim; Y means sulfur or oxygen atom; Z means oxygen atom. EFFECT: broadened arsenal of agents of indicated prescription. 4 tbl, 10 ex

公开(公告)号：RU2180335C2

公开(公告)日：2002-03-10

申请号：RU97107617

申请日：1995-10-07

Applicant: BASF AG

Inventor： KHARTMUT RIKHERS ,  DAGMAR KLINGE ,  VIL KHEL M AMBERG ,  ANDREAS KLING ,  SHTEFAN MJULLER ,  EHRNST BAUMANN ,  JOAKHIM RAJNKHAJMER ,  UVE JOZEF FOGEL BAKHER ,  VOL FGANG VERNET ,  LILIANE UNGER ,  MANFRED RASHAK

IPC: C07D251/30 ,  A61K31/505 ,  A61P9/00 ,  A61P9/08 ,  A61P9/10 ,  A61P9/12 ,  A61P11/08 ,  A61P13/02 ,  A61P15/00 ,  A61P25/04 ,  C07D239/00 ,  C07D239/26 ,  C07D239/28 ,  C07D239/34 ,  C07D239/38 ,  C07D239/60 ,  C07D239/70 ,  C07D239/96 ,  C07D251/12 ,  C07D251/52 ,  C07D257/02 ,  C07D309/00 ,  C07D403/06 ,  C07D403/12 ,  C07D405/12 ,  C07D417/12 ,  C07D487/04 ,  C07D491/04 ,  C07D491/044 ,  C07D491/048

Abstract: organic synthesis. SUBSTANCE: invention provides novel carboxylic acid derivatives having general formula I: (I) and containing heterocyclic moieties. Compound possess biological activity, in particular they inhibit binding of endothelin to receptors and can be used for treatment of hypertension, myocardial infarction, renal insufficiency, and other maladies. In the formula I, (i) R1 denotes tetrazole, nitrile, carboxylic group, group COOR7, in which R7 is C1-C4-alkyl or alkali of alkaliearth cation, group -CONHSO2R8, in which R8 is C1-C4-alkyl, or group -CONHSO2R9, in which R9 is C1-C4-alkyl; (ii) R2 denotes hydroxy group, amino group, di-C1-C4- alkylaino group, or C1-C4-alkoxy group; (iii) X denotes nitrogen or radical CR10, in which R10 is hydrogen or C1-C5- alkyl, or CR10 and CR3 together form 5- or 6-membered alkylene or alkenylene ring optionally substituted by 1 or 2 C1- C4-alkyl group and in which one methylene group can be substituted by oxygen, imino or C1-C4-imino group; (iv) R3 denotes mono- or di-C1-C4-alkyl group, C1- C4-alkyl, C1-C4-alkoxy, or CR3 together with CR10 form above-described ring; (v) R4 and R5 each denote phenyl optionally substituted by halogen, C1-C4-alkyl or C1-C4-alkoxy, provided that two phenyls are in ortho-position to each other and linked by an ordinary linkage, methylene or ethylene group, or C3- C7- cycloalkyl group; (vi) R6 denotes C1-C8-alkyl or C3-C6-alkenyl optionally substituted by halogen, cyano, C1-C4- alkoxy, C1-C4-alkylthio, or phenyl; phenyl optionally substituted by one or two groups selected from halogen, C1-C4- alkyl, C1-C4-alkoxyl; cycloalkyl optionally substituted by C1-C4-alkyl; or five- or six-membered heterocyclic residue containing one sulfur or oxygen atom and optionally substituted by C1-C4-alkyl; and (vii) Z denotes sulfur, oxygen, sulfinyl or sulfonyl. EFFECT: extended choice of drugs. 3 tbl, 25 ex