公开(公告)号：NZ504316A

公开(公告)日：2002-12-20

申请号：NZ50431698

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 ,  C07D239/26 ,  C07D491/052 ,  C07D491/056 ,  C07D413/12

Abstract: A carboxylic acid derivative of formula (I) or a salt wherein: R1 is tetrazole or -C(O)-R; R is OR9, a 5-membered heteroaromatic ring system linked via a nitrogen atom; -O-(CH2)p-S(O)k-R10 or -NH-SO2-R11; R2 is H, OH, NH2, NH-alkyl, N(alkyl)2, halogen, alkyl, alkenyl, alkynyl, haloalkyl, alkoxy, haloalkoxy or alkylthio or CR2 is linked to CR12 to give a 5 or 6- membered ring; X is nitrogen or methine and Y is nitrogen or methine; Z is nitrogen or CR12 wherein two of X to Z are nitrogen and the other is methine of CR12; R3 is H, OH, NH2, NH-alkyl, N(alkyl)2, halogen, alkyl, alkenyl, alkynyl, haloalkyl, alkoxy, haloalkoxy or alkylthio or CR3 is linked to CR12 to give a 5 or 6- membered ring R4 and R5 are independently cycloalkyl; optionally substituted phenyl or naphthyl, which can be connected together in the ortho positions by a direct linkage, methylene, ethylene or ethenylene, oxygen, sulphur, SO2, NH or N-alkyl; R3 is -C(O)-NR13R14 or -C(R21)(R20)-N(R18)(R19); R7 and R8 are independently H or alkyl; W is O or S and the rest of the variables are as defined in the specification. The compound can be in enantiomerically pure or diastereomerically pure form and is useful for treating diseases where an endothelin level is elevated.

公开(公告)号：AU748610B2

公开(公告)日：2002-06-06

申请号：AU9533398

申请日：1998-08-24

Applicant: BASF AG

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

IPC: A61K31/421 ,  A61K31/426 ,  A61K31/428 ,  A61K31/496 ,  A61K31/505 ,  A61P9/10 ,  A61P9/12 ,  A61P43/00 ,  C07D239/34 ,  C07D239/52 ,  C07D263/38 ,  C07D277/20 ,  C07D277/34 ,  C07D277/68 ,  C07D409/12 ,  C07D239/04

Abstract: The invention relates to carboxylic acid derivatives of formula (I) wherein the radicals are defined in the description, and to the use of these derivatives as ETA/ETB endothelin-receptor antagonists.

公开(公告)号：SK11752000A3

公开(公告)日：2001-05-10

申请号：SK11752000

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：AU731579B2

公开(公告)日：2001-04-05

申请号：AU2636597

申请日：1997-04-04

Applicant: BASF AG

Inventor： KLINGE DAGMAR ,  AMBERG WILHELM ,  BAUMANN ERNST ,  KLING ANDREAS ,  RIECHERS HARTMUT ,  UNGER LILIANE ,  RASCHACK MANFRED ,  HERGENRODER STEFAN ,  SCHULT SABINE

IPC: A61K31/00 ,  A61K31/505 ,  A61K31/517 ,  A61P5/42 ,  A61P9/10 ,  A61P13/00 ,  A61P13/12 ,  C07D217/22 ,  C07D239/34 ,  C07D239/48 ,  C07D239/52 ,  C07D239/56 ,  C07D239/60 ,  C07D239/70 ,  C07D239/80 ,  C07D239/96 ,  C07D251/20 ,  C07D251/22 ,  C07D251/30 ,  C07D251/38 ,  C07D251/52 ,  C07D403/12 ,  C07D405/12 ,  C07D471/04 ,  C07D487/04 ,  C07D491/04 ,  C07D491/044

Abstract: The present invention relates to carboxylic acid derivatives of the formulawhere the radicals have the meanings stated in the description, to the preparation of these compounds and to their use as drugs.

公开(公告)号：NZ336157A

公开(公告)日：2000-10-27

申请号：NZ33615797

申请日：1997-12-04

Applicant: BASF AG

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

IPC: C07D253/06 ,  A61K31/495 ,  A61K31/50 ,  A61K31/505 ,  A61K31/53 ,  A61P9/10 ,  A61P9/12 ,  A61P11/06 ,  A61P13/08 ,  C07D237/14 ,  C07D237/16 ,  C07D241/18 ,  C07D253/07 ,  C07D253/075 ,  C07D253/10 ,  C07D403/12 ,  C07D491/04 ,  C07D241/20 ,  C07D237/20 ,  C07D253/08 ,  C07D237/18 ,  C07D237/22

Abstract: Carboxylic acid derivatives of formula I, wherein R1, R2, R3, R4 and R5 are as described in the specification, X is nitrogen or methane; with the proviso that if x = nitrogen then z = nitrogen and if x = methane then at least one of the ring members Y or Z is nitrogen. Y is nitrogen or CR9 Z is nitrogen or CR10 R9 and R10 (which can be identical or different) are: hydrogen, hydroxyl, NH2, NH(C1-C4-alkyl), N(C1-C4-alkyl)2, halogen, C1-C4-alkyoxy, C1-C4-haloalkoxy or C1-C4-alkylthio; C1-C4-alkyl, C2-C4-alkenyl, C2-C4-alkynyl; or CR9 or CR10 is linked with CR2 as indicated above to give a 5 or 6 membered ring. W is sulfur, oxygen or a single bond Q is oxygen or nitrogen, with the proviso that if Q = nitrogen then W is a singe bond. Also disclosed is the use of formula one as an endothelin receptor antagonist and its use in the treatment of illnesses in which raised endothelin levels occur. Such illnesses include the treatment of cardiac insufficiency, restenosis, high blood pressure, acute/chronic kidney failure and prostate cancer.

公开(公告)号：NZ332096A

公开(公告)日：2000-01-28

申请号：NZ33209697

申请日：1997-04-04

Applicant: BASF AG

Inventor： KLINGE DAGMAR ,  AMBERG WILHELM ,  BAUMANN ERNST ,  KLING ANDREAS ,  RIECHERS HARTMUT ,  UNGER LILIANE ,  RASCHACK MANFRED ,  HERGENRODER STEFAN ,  SCHULT SABINE

IPC: A61K31/00 ,  A61K31/505 ,  A61K31/517 ,  A61P5/42 ,  A61P9/10 ,  A61P13/00 ,  A61P13/12 ,  C07D217/22 ,  C07D239/34 ,  C07D239/48 ,  C07D239/52 ,  C07D239/56 ,  C07D239/60 ,  C07D239/70 ,  C07D239/80 ,  C07D239/96 ,  C07D251/20 ,  C07D251/22 ,  C07D251/30 ,  C07D251/38 ,  C07D251/52 ,  C07D403/12 ,  C07D405/12 ,  C07D471/04 ,  C07D487/04 ,  C07D491/04 ,  C07D491/044 ,  C07D239/95 ,  C07D491/052 ,  C07D239/86 ,  C07D239/46 ,  C07D491/056 ,  A61K31/53

Abstract: isclosed are carboxylic acid derivatives of the formula (I) in which the radicals have the meaning given in the description, the production of these compounds and their use as medicaments.

公开(公告)号：ID19050A

公开(公告)日：1998-06-04

申请号：ID971240

申请日：1997-04-14

Applicant: BASF AG

Inventor： AMBERG WILHELM ,  KLING ANDREAS ,  KLINGE DAGMAR ,  RIECHERS HARTMUT ,  BAUMANN ERNST ,  UNGER LILIANE ,  RASCHACK MANFRED ,  HERGENRODER STEFAN ,  SCHULT SABINE

IPC: A61K31/00 ,  A61K31/47 ,  A61K31/505 ,  A61P9/00 ,  A61P9/12 ,  A61P13/00 ,  A61P13/12 ,  C07D215/22 ,  C07D215/227 ,  C07D239/34 ,  C07D239/60 ,  C07D401/12 ,  C07D403/12 ,  C07D247/00

Abstract: PCT No. PCT/EP97/01687 Sec. 371 Date Oct. 8, 1998 Sec. 102(e) Date Oct. 8, 1998 PCT Filed Apr. 4, 1997 PCT Pub. No. WO97/38982 PCT Pub. Date Oct. 23, 1997Carboxylic acid derivatives of the formula I where the radicals have the meanings stated in the description, and the preparation of these agreements [sic] and their use as drugs are described.

公开(公告)号：ID16501A

公开(公告)日：1997-10-02

申请号：ID971242

申请日：1997-04-14

Applicant: BASF AG

Inventor： KLINGE DAGMAR ,  AMBERG WILHELM ,  BAUMANN ERNEST ,  KLING ANDREAS ,  RIECHERS HARTMUT ,  UNGER LILIANNE ,  RASCHACK MANFRED ,  HERGENRODER STEFAN ,  SCHULT SABINE

IPC: A61K31/00 ,  A61K31/505 ,  A61K31/517 ,  A61P5/42 ,  A61P9/10 ,  A61P13/00 ,  A61P13/12 ,  C07D217/22 ,  C07D239/34 ,  C07D239/48 ,  C07D239/52 ,  C07D239/56 ,  C07D239/60 ,  C07D239/70 ,  C07D239/80 ,  C07D239/96 ,  C07D251/20 ,  C07D251/22 ,  C07D251/30 ,  C07D251/38 ,  C07D251/52 ,  C07D403/12 ,  C07D405/12 ,  C07D471/04 ,  C07D487/04 ,  C07D491/04 ,  C07D491/044

Abstract: The present invention relates to carboxylic acid derivatives of the formulawhere the radicals have the meanings stated in the description, to the preparation of these compounds and to their use as drugs.

公开(公告)号：CZ20012186A3

公开(公告)日：2002-07-17

申请号：CZ20012186

申请日：1999-12-09

Applicant: BASF AG

Inventor： AMBERG WILJHEM ,  JANSEN ROLF ,  KETTSCHAU GEORG ,  RIECHERS HARTMUT ,  BAUMANN ERNST ,  HERGENRODER STEFAN ,  RASCHACK MANFRED ,  UNGER LILIANE

IPC: C07D251/24 ,  A61K31/505 ,  A61K31/506 ,  A61K31/53 ,  A61P9/04 ,  A61P9/10 ,  A61P9/12 ,  A61P13/08 ,  A61P13/12 ,  A61P15/10 ,  A61P35/00 ,  A61P43/00 ,  C07C229/34 ,  C07C233/87 ,  C07C235/52 ,  C07D239/34 ,  C07D251/22 ,  C07D401/12 ,  C07D491/048 ,  C07D403/12 ,  A61P9/00 ,  A61P13/00

Abstract: The invention relates to carboxylic acid derivatives of formula (I), in which the substituents have the following meanings: R is tetrazol or a group (a); W and Z, can be identical or different and are nitrogen or methine, provided that if W and Z are methine, then Q is nitrogen; X is nitrogen or CR ; Y is nitrogen or CR ; Q is nitrogen or CR , provided that if Q is nitrogen then X is CR and Y is CR ; R and R are identical or different and are possibly substituted phenyl or naphthyl or phenyl or naphthyl which are linked in an ortho position via a direct bond, a methlyene, ethylene or ethenylene group, an oxygen or sulfur atom or a SO2-, NH- or N-alkyl group or possibly substituted C5-C6-cycloalkyl; R is a rest (b) or (c); and R is hydrogen, C1-C4-alkyl. The invention further relates to their preparation and their use as endothelin receptor antagonists. The invention also relates to compounds of formula (II) and a structural fragment of formula (d) in which the rests R , R , R , R and R have the meanings given in claim no. 1 and to their use as structural elements in an endothelin receptor antagonist.

公开(公告)号：NZ504289A

公开(公告)日：2002-03-01

申请号：NZ50428998

申请日：1998-11-04

Applicant: BASF AG

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

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 ,  A61P9/00

Abstract: Carboxylic acid derivatives of formula I, and their preparation and use as endothelin receptor antagonists.