公开(公告)号：AU3408799A

公开(公告)日：1999-09-20

申请号：AU3408799

申请日：1999-02-25

Applicant: BASF AG

Inventor： AMBERG WILHELM ,  JANSEN ROLF ,  KLINGE DAGMAR

IPC: C07D239/38 ,  A61K31/19 ,  A61K31/215 ,  A61K31/357 ,  A61K31/36 ,  A61K31/505 ,  A61P43/00 ,  C07C319/14 ,  C07C323/56 ,  C07D239/56 ,  C07D239/60 ,  C07D317/62 ,  C07C323/00

Abstract: A process for preparing endothelin receptor antagonists of the sulfanyl type of the general formula Iby nucleophilic reaction of a carboxylic acid derivative of the formula II with a sulfide of the formula IIIto give endothelin receptor antagonists of the formula I.

公开(公告)号：AU2624799A

公开(公告)日：1999-09-20

申请号：AU2624799

申请日：1999-02-25

Applicant: BASF AG

Inventor： AMBERG WILHELM ,  JANSEN ROLF ,  KLINGE DAGMAR ,  RIECHERS HARTMUT ,  HERGENRODER STEFAN ,  RASCHACK MANFRED ,  UNGER LILIANE

IPC: C07D251/22 ,  A61K31/192 ,  A61K31/216 ,  A61K31/505 ,  A61K31/506 ,  A61K31/519 ,  A61K31/53 ,  A61P9/04 ,  A61P9/06 ,  A61P9/10 ,  A61P9/12 ,  A61P11/06 ,  A61P13/08 ,  A61P13/12 ,  A61P35/00 ,  A61P43/00 ,  C07C59/66 ,  C07C59/68 ,  C07C69/734 ,  C07D213/63 ,  C07D239/34 ,  C07D239/52 ,  C07D239/60 ,  C07D405/12 ,  C07D491/048 ,  C07D403/12 ,  C07D213/64

Abstract: The invention relates to carboxylic acid derivatives of formula (I), wherein R -R , Q, W, X, Y and Z have the meanings given in the description. The novel compounds are suitable for combating diseases.

公开(公告)号：CA2322226A1

公开(公告)日：1999-09-10

申请号：CA2322226

申请日：1999-02-25

Applicant: BASF AG

Inventor： AMBERG WILHELM ,  JANSEN ROLF ,  KLINGE DAGMAR

IPC: C07D239/38 ,  A61K31/19 ,  A61K31/215 ,  A61K31/357 ,  A61K31/36 ,  A61K31/505 ,  A61P43/00 ,  C07C319/14 ,  C07C323/56 ,  C07D239/56 ,  C07D239/60 ,  C07D317/62 ,  C07C323/22 ,  C07D317/56

Abstract: The invention relates to a method for preparing sulfanyl-type endothelin receptor antagonists of general formula (I) wherein R1 represents hydroxy, alkoxy, sulfonamidyl, amino; R2 represents alkyl, aryl or heteroaryl, optionally substituted, and R3, R4, R5 can be the same or different and are alkyl or aryl, optionally substituted, by means of nucleophilic reaction of a carboxylic acid derivative of formula (II) with a sulfide of formula (III), X being SR6 or SO2R6 and R6 being alkyl or aryl, optionally substituted.

公开(公告)号：DE19809635A1

公开(公告)日：1999-09-09

申请号：DE19809635

申请日：1998-03-06

Applicant: BASF AG

Inventor： AMBERG WILHELM ,  JANSEN ROLF ,  KLINGE DAGMAR

IPC: C07D239/38 ,  A61K31/19 ,  A61K31/215 ,  A61K31/357 ,  A61K31/36 ,  A61K31/505 ,  A61P43/00 ,  C07C319/14 ,  C07C323/56 ,  C07D239/56 ,  C07D239/60 ,  C07D317/62 ,  C07B45/06 ,  C07D239/46 ,  C07D319/06 ,  C07C323/50

Abstract: The invention relates to a method for preparing sulfanyl-type endothelin receptor antagonists of general formula (I) wherein R represents hydroxy, alkoxy, sulfonamidyl, amino; R represents alkyl, aryl or heteroaryl, optionally substituted, and R , R , R can be the same or different and are alkyl or aryl, optionally substituted, by means of nucleophilic reaction of a carboxylic acid derivative of formula (II) with a sulfide of formula (III), X being SR or SO2R and R being alkyl or aryl, optionally substituted.

公开(公告)号：BG102362A

公开(公告)日：1999-08-31

申请号：BG10236298

申请日：1998-04-01

Applicant: BASF AG

Inventor： KLINGE DAGMAR ,  AMBERG WILHELM ,  KLING ANDREAS ,  RIECHERS HARTMUT ,  UNGER LILIANE ,  RASCHACK MANFRED

IPC: A61K31/00 ,  A61K31/44 ,  A61K31/4427 ,  A61K31/443 ,  A61K31/444 ,  A61K31/505 ,  A61K31/53 ,  A61P5/24 ,  A61P5/36 ,  A61P5/42 ,  A61P9/12 ,  C07D213/74 ,  C07D239/10 ,  C07D239/42 ,  C07D239/46 ,  C07D239/48 ,  C07D239/50 ,  C07D239/52 ,  C07D239/58 ,  C07D251/46 ,  C07D401/04 ,  C07D405/12 ,  C07D405/14 ,  C07D471/04 ,  C07D487/04 ,  C07D491/052 ,  C07D491/056 ,  C07D239/70 ,  C07D487/02 ,  C07D251/42

Abstract: The invention relates to derivatives of aminoacids with theformulawhere the radicals have the meanings listed in the description, aswell as to their use as medicamentous forms.4 claims

公开(公告)号：DE19806438A1

公开(公告)日：1999-08-19

申请号：DE19806438

申请日：1998-02-17

Applicant: BASF AG

Inventor： AMBERG WILHELM ,  JANSEN ROLF ,  KLING ANDREAS ,  KLINGE DAGMAR ,  RIECHERS HARTMUT ,  HERGENROEDER STEFAN ,  RASCHACK MANFRED ,  UNGER LILIANE

IPC: A61K31/505 ,  A61K31/506 ,  A61P5/14 ,  A61P9/02 ,  A61P9/10 ,  A61P9/12 ,  A61P11/06 ,  A61P13/12 ,  A61P35/00 ,  A61P43/00 ,  C07D239/34 ,  C07D239/46 ,  C07D239/52 ,  C07D239/60 ,  C07D401/12 ,  C07D403/12 ,  C07D405/12 ,  C07D409/12 ,  C07D417/12

Abstract: Pyrimidinyloxy-propionic acid derivatives (I) are new. Also new are combinations of (I) with inhibitors of the renin-angiotensin system, beta -blockers, diuretics, calcium antagonists and VEGF blockers. (Pyrimidin-2-yloxy)-propionic acid derivatives of formula (I) and their salts are new: R = tetrazolyl or C(O)R; R = OR , N-bonded heteroaryl optionally substituted with halo, alkyl or alkoxy, -O-(CH2)p-S(O)k-R or -NH-SO2-R ; R = H, an alkali or alkaline earth cation, NH4 , an organic ammonium ion, cycloalkyl, alkyl, optionally substituted benzyl, optionally halogenated alkenyl or alkynyl or optionally substituted phenyl; R = alkyl, cycloalkyl, alkenyl, alkynyl or optionally substituted phenyl; k = 0-2; p = 1-4; R = optionally substituted alkyl, alkenyl, alkynyl, cycloalkyl or phenyl; R = H, OH, NH2, NH(alkyl), N(alkyl)2, halo, alkyl, alkenyl, alkynyl, hydroxyalkyl, haloalkyl, alkoxy, haloalkoxy, alkylthio or morpholinyl; X = halo, haloalkyl or OH; R = H, OH, NH2, NH(alkyl), N(alkyl)2, halo, alkyl, alkenyl, alkynyl, hydroxyalkyl, haloalkyl, alkoxy, haloalkoxy, -NH-O-alkyl or alkylthio; R , R = optionally substituted phenyl or naphthyl; phenyl or naphthyl ortho-linked with one another via a bond, methylene, ethylene, ethenylene, O, S, SO2, NH or N(alkyl); optionally substituted heteroaryl; or cycloalkyl; Z' = S, O, or a single bond; and R = H (when Z = S or O), optionally substituted alkyl, alkenyl, alkynyl, cycloalkyl, phenyl, naphthyl or heteroaryl. The full definitions are given in the DEFINITIONS (Full Definitions) Field. An Independent claim is also included for combinations of (I) with inhibitors of the renin-angiotensin system, beta -blockers, diuretics, calcium antagonists and VEGF blockers.

公开(公告)号：AU1487899A

公开(公告)日：1999-06-07

申请号：AU1487899

申请日：1998-11-04

Applicant: BASF AG

Inventor： AMBERG WILHELM ,  JANSEN ROLF ,  HILLEN HEINZ ,  HERGENRODER STEFAN ,  RASCHACK MANFRED ,  UNGER LILIANE

IPC: C07D249/12 ,  A61K31/41 ,  A61K31/415 ,  A61K31/4164 ,  A61K31/42 ,  A61K31/421 ,  A61K31/422 ,  A61K31/4245 ,  A61K31/425 ,  A61K31/426 ,  A61K31/427 ,  A61K31/428 ,  A61K31/433 ,  A61P9/04 ,  A61P9/08 ,  A61P9/10 ,  A61P9/12 ,  A61P11/06 ,  A61P13/08 ,  A61P13/12 ,  A61P35/00 ,  A61P43/00 ,  C07D231/20 ,  C07D233/70 ,  C07D261/12 ,  C07D263/38 ,  C07D271/06 ,  C07D271/10 ,  C07D273/01 ,  C07D275/02 ,  C07D275/03 ,  C07D277/20 ,  C07D277/32 ,  C07D277/34 ,  C07D277/60 ,  C07D277/68 ,  C07D285/00 ,  C07D285/08 ,  C07D285/12 ,  C07D291/04 ,  C07D413/12 ,  C07D417/12

Abstract: The present invention relates to carboxylic acid derivatives of the formula Ithe substituents having the meanings explained in the description, preparation and use as endothelin receptor antagonists.

公开(公告)号：CO4790169A1

公开(公告)日：1999-05-31

申请号：CO99013759

申请日：1999-03-05

Applicant: BASF AG

Inventor： AMBERG WILHELM ,  JANSEN ROLF ,  KLINGE DAGMAR

IPC: C07D239/38 ,  A61K31/19 ,  A61K31/215 ,  A61K31/357 ,  A61K31/36 ,  A61K31/505 ,  A61P43/00 ,  C07C319/14 ,  C07C323/56 ,  C07D239/56 ,  C07D239/60 ,  C07D253/00 ,  C07D317/62 ,  C03C303/26

Abstract: Procedimiento para la obtención de derivados de ácidocarboxílico de la fórmula general I:en la que R1 significa hidroxi, alcoxi, sulfonamidilo, amino, R2 significa alquilo, arilo o heteroarilo, eventualmente sustituido, R3 , R4 , R5 son idénticos o diferentes ysignifican independientemente alquilo o arilo, eventualmente sustituido. Por reacción nucleófila de un derivado de ácido carboxílico de la fórmula II con un sulfuro de la fórmula III en la que X significa SR6 o SO2 R6 R6 significa alquilo o arilo, eventualmente sustituido.

公开(公告)号：AU2266199A

公开(公告)日：1999-05-24

申请号：AU2266199

申请日：1998-10-16

Applicant: BASF AG

Inventor： AMBERG WILHELM ,  JANSEN ROLF ,  HERGENRODER STEFAN ,  RASCHACK MANFRED ,  UNGER LILIANE

IPC: A61K31/505 ,  A61K31/506 ,  A61K31/517 ,  A61K31/519 ,  A61K31/5377 ,  A61P9/02 ,  A61P9/10 ,  A61P9/12 ,  A61P13/08 ,  A61P13/12 ,  A61P35/00 ,  A61P43/00 ,  C07D239/34 ,  C07D239/36 ,  C07D239/52 ,  C07D239/60 ,  C07D239/70 ,  C07D401/12 ,  C07D403/12 ,  C07D491/048 ,  C07D239/00

Abstract: The invention relates to carboxylic acid derivatives of formula (I), wherein the substituents have the meaning as commented in the description. It also relates to the production and use of same as endothelin receptor antagonists.

公开(公告)号：NO991079A

公开(公告)日：1999-05-04

申请号：NO991079

申请日：1999-03-04

Applicant: BASF AG

Inventor： AMBERG WILHELM ,  JANSEN ROLF ,  KLING ANDREAS ,  KLINGE DAGMAR ,  RIECHERS HARTMUT ,  HERGENR DER STEFAN ,  RASCHACK MANFRED ,  UNGER LILIANE

IPC: A61K31/505 ,  A61K31/506 ,  A61K31/519 ,  A61P9/04 ,  A61P9/08 ,  A61P9/12 ,  A61P43/00 ,  C07C59/66 ,  C07C69/734 ,  C07D239/34 ,  C07D239/52 ,  C07D239/60 ,  C07D239/70 ,  C07D491/04 ,  C07D491/048

CPC classification number: C07D239/70 ,  C07C59/66 ,  C07C69/734 ,  C07D239/34 ,  C07D239/52 ,  C07D239/60 ,  C07D491/04