公开(公告)号：BG104396A

公开(公告)日：2001-02-28

申请号：BG10439600

申请日：2000-05-02

Applicant: BASF AG

Inventor： AMBERG WILHELM ,  JANSEN ROLF ,  HERGENROEDER 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

Abstract: The invention relates to derivatives of carboxylic acids with the formula wherein R6 is the group or R13 and R14 are the same or different meaning hydrogen provided that R13 and R14 are not simultaneously hydrogen, C1-C8-alkyl, C3-C8-cycloalkyl, C3-C8-alkenyl, C3-C8-alkynyl, benzyl, phenyl, naphthyl, optionally substituted, or R13 and R14 together form a closed in a ring C3-C7-alkylene chain, optionally substituted, and in which an alkylene group can be substituted with oxygen, sulphur, nitrogen, or R13 and R14 together form a closed in a ring C3-C7-alkylene chain, or C4-C7-alkenyl chain, optionally substituted, which can be with a phenyl ring, optionally substituted. The remaining substituents have the meanings given in the description. The invention also relates to new derivatives of carboxylic acids and to their use as endothelin-receptor antagonists. 14 claims

公开(公告)号：AU6561500A

公开(公告)日：2001-02-05

申请号：AU6561500

申请日：2000-07-05

Applicant: BASF AG

Inventor： AMBERG WILHELM ,  KETTSCHAU GEORG

IPC: A61K31/505 ,  A61K31/506 ,  A61K31/517 ,  A61P1/18 ,  A61P5/16 ,  A61P9/00 ,  A61P9/04 ,  A61P9/10 ,  A61P9/12 ,  A61P11/00 ,  A61P11/06 ,  A61P13/00 ,  A61P13/12 ,  A61P35/00 ,  A61P43/00 ,  C07D239/34 ,  C07D239/47 ,  C07D239/52 ,  C07D239/56 ,  C07D239/70 ,  C07D239/80 ,  C07D401/12 ,  C07D405/12 ,  C07D409/12 ,  C07D473/28 ,  C07D403/12

Abstract: The invention relates to compounds of formula (I), whereby the substituents have the meaning cited in the description. The invention also relates to the utilization of said derivatives.

公开(公告)号：AU729333B2

公开(公告)日：2001-02-01

申请号：AU7495796

申请日：1996-10-30

Applicant: BASF AG

Inventor： KLING ANDREAS ,  JANSSEN BERND ,  AMBERG WILHELM ,  HAUPT ANDREAS ,  RITTER KURT ,  BUSCHMANN ERNST ,  BERNARD HARALD ,  MULLER STEFAN ,  ZIERKE THOMAS ,  BARLOZZARI TERESA ,  ARRUDA MONIKA DE ,  ROBINSON SIMON

IPC: A61K38/00 ,  A61K31/00 ,  C07K7/06 ,  A61K38/08

Abstract: Novel peptides of the formulaA-B-D-E-F-L,wherein A, B, D, E, F, and L have the meanings stated in the specification, and their preparation are disclosed. The novel compounds are suitable for controlling diseases.

公开(公告)号：SK12012000A3

公开(公告)日：2001-01-18

申请号：SK12012000

申请日：1999-02-25

Applicant: BASF AG

Inventor： AMBERG WILHELM ,  JANSEN ROLF ,  KLINGE DAGMAR

IPC: A61K31/19 ,  A61K31/215 ,  C07D239/38 ,  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：TR200002376T2

公开(公告)日：2000-12-21

申请号：TR200002376

申请日：1999-02-05

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: The invention relates to carboxylic acid derivatives of formula (I), wherein the substituents have the following meanings; R = tetrazole or a group (1); R = a radical OR (2), (3), a 5-membe red heteroaromatic bonded by a nitrogen atom such a pyrrolyl, pyrazolyl, imidazolyl and trizolyl; R , R = hydrogen, hydroxy, NH2, NH(C1-C4-alkyl), N(C1-C4-alkyl)2, halogen, C1-C4-alkyl, C2-C4-alkenyl, C2-C4-alkinyl, C1-C4-hydroxyalkyl, C1-C4-alkoxy, C1-C4-halogen alkyl, C1-C4-alkoxy, C1-C4-halogen alkoxy or C1-C4-alkythio; X = halogen, C1-C4-halogen alkyl, hydroxy; R and R = phenyl or naphthyl, C3-C7-cycloalkyl, phenyl or naphthyl which are bonded in ortho position by a direct bond, a methylene, ethylene or ethenylene group, an oxygen or sulfur atom or an SO2-NH or an N-alkyl group or a 5-membered or 6-membered heteroaromatic; R = hydrogen, phenyl or naphthyl, a five or six-membered heteroaromatic, C1-C8-alkyl, C3-C6-alkenyl, C3-C6-alkinyl or C3-C8-cycloalkyl, whereby said radicals can be substituted once or many times, with the proviso that R can only stand for hydrogen if Z does not represent a single bond; Z = sulfur, oxygen or a single bond, in addition to the physiologically compatible salts and the enantiomeric-pure and diastereomeric-pure forms. The novel compounds are suitable for combating diseases, especially as endothelin antagonists.

公开(公告)号：AU5395900A

公开(公告)日：2000-12-18

申请号：AU5395900

申请日：2000-05-19

Applicant: BASF AG

Inventor： AMBERG WILHELM ,  KETTSCHAU GEORG

IPC: C07D251/14 ,  A61K31/4418 ,  A61K31/50 ,  A61K31/505 ,  A61K31/517 ,  A61K31/519 ,  A61K31/53 ,  A61K45/00 ,  A61P9/00 ,  A61P9/04 ,  A61P9/10 ,  A61P9/12 ,  A61P11/06 ,  A61P13/08 ,  A61P35/00 ,  C07D213/64 ,  C07D213/68 ,  C07D237/14 ,  C07D239/34 ,  C07D239/52 ,  C07D251/30 ,  C07D253/06 ,  C07D239/00

Abstract: The invention relates to carboxylic acid derivatives of formula (I), whereby the substituents have the meanings as explained in the description. The invention also relates to the production and use of said novel carboxylic acid derivatives as endothelin receptor antagonists.

公开(公告)号：BR9908585A

公开(公告)日：2000-11-21

申请号：BR9908585

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：BR9908401A

公开(公告)日：2000-10-31

申请号：BR9908401

申请日：1999-02-25

Applicant: BASF AG

Inventor： AMBERG WILHELM ,  JANSEN ROLF ,  KLINGE DAGMAR ,  RIECHERS HARMUT ,  DER STEFAN HERGENR ,  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：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：TR199802042T2

公开(公告)日：2000-09-21

申请号：TR9802042

申请日：1997-04-04

Applicant: BASF AG

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

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.