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：RU2167869C2

公开(公告)日：2001-05-27

申请号：RU97102158

申请日：1995-07-14

Applicant: BASF AG

Inventor： BEATE KHELLENDAL ,  ANNEGRET LANSKI ,  RAJNER MUNSHAUER ,  ZIGFRID BIALOJAN ,  LILIANE UNGER ,  KHANS-JURGEN TESHENDORF ,  KARSTEN VIKE ,  KARLA DRESHER

IPC: C07D249/08 ,  A61K31/41 ,  A61K31/435 ,  A61K31/4427 ,  A61K31/445 ,  A61K31/505 ,  A61K31/53 ,  A61P1/08 ,  A61P25/18 ,  A61P25/20 ,  A61P25/24 ,  A61P25/26 ,  C07D249/12 ,  C07D249/14 ,  C07D401/06 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D403/14

Abstract: organic chemistry, pharmacy. SUBSTANCE: invention relates to novel compounds of triazole of the general formula (I) where A means linear or branched C1-C18-alkylene group that can include at least one group that is taken among O, S, CONH, COO, C3-C6-cycloalkylene or double or triple bond; B means radical of the formula (a) , (b) or (c) ; R1 means H, NH2, C3-C6-cycloalkyl or C1-C8-alkyl that can be free or substituted with O-C1-C8-alkyl; R2 means H, OH, C1-C8-alkyl, C3-6-cycloalkyl, CF3, CN, WR3R4,SR3 or CO2R3 where R3 means H or C1-C8-alkyl and R4 means H, C1-C8-alkyl or COR3 where R34 means C1-C8-alkyl; Ar means naphthyl, phenyl with 1-2 substituents taken among C1-C8-alkyl, CF3,CHF2,NO2,SR3,SO2R3 where R3 means C1-C8-alkyl and also pyridyl, pyrimidyl or triazinyl that have from 1 to 3 substituents taken among C1-C8-alkyl, C2-C6-alkenyl, C2-C6/ -alkynyl, halogen atom, CN, CF3,OR4 where R4 means hydrogen atom or C1-C8-alkyl, CO2R3 where R3 means C1-C8-alkyl, phenyl that can be substituted with halogen atom, alkoxy- or phenoxy-group, C3-C6-cycloalkyl that can be condensed, phenylalkylamine or 5-membered aromatic heterocycle with 1-2 nitrogen atoms that can be condensed with benzene ring. Compounds show high affinity to dophamine-D3-[sic] -receptors and therefore they can be used for treatment of patients with disorders giving responses for dophamine-D3-ligands. Invention describes also pharmaceutical composition based on compounds of the formula (I). EFFECT: new compounds, valuable pharmacological properties. 11 cl, 9 tbl