公开(公告)号：BG106154A

公开(公告)日：2002-08-30

申请号：BG10615401

申请日：2001-11-27

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

Abstract: The invention relates to carboxylic acid derivatives of formula whereby the substituents have the meanings as explained in the description. The invention also relates to production and use of said novel carboxylic acid derivatives as endothelin receptor antagonists. 8 claims

公开(公告)号：SK8682001A3

公开(公告)日：2002-08-06

申请号：SK8682001

申请日：1999-12-09

Applicant: BASF AG

Inventor： AMBERG WILHELM ,  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 ,  C07D239/60

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：NO312674B1

公开(公告)日：2002-06-17

申请号：NO991079

申请日：1999-03-04

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 ,  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 ,  C07D237/34

Abstract: The invention relates to carboxylic acid derivatives of the formula Iwhere the radicals have the meanings stated in the description, and to their use as drugs.

公开(公告)号：HU0104007A2

公开(公告)日：2002-05-29

申请号：HU0104007

申请日：1999-08-07

Applicant: BASF AG

Inventor： AMBERG WILHELM ,  HERGENROEDER STEFAN ,  JANSEN ROLF ,  KETTSCHAU GEORG ,  RASCHACK MANFRED ,  UNGER LILIANE

IPC: C07D251/22 ,  A61K31/505 ,  A61K31/517 ,  A61K31/519 ,  A61K31/53 ,  A61K45/00 ,  A61P9/04 ,  A61P9/10 ,  A61P9/12 ,  A61P13/08 ,  A61P13/12 ,  A61P35/00 ,  A61P43/00 ,  C07D239/34 ,  C07D239/52 ,  C07D239/60 ,  C07D239/70 ,  C07D251/52 ,  C07D401/12 ,  C07D403/12 ,  C07D405/12 ,  C07D491/048 ,  C07D495/04

Abstract: The invention relates to new carboxylic acid derivatives of the formula (I), where the substituents have the meaning given in the description, their production and their use as endothelin-receptor antagonists.

公开(公告)号：BR0012592A

公开(公告)日：2002-05-28

申请号：BR0012592

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：ZA200101975B

公开(公告)日：2002-03-11

申请号：ZA200101975

申请日：2001-03-09

Applicant: BASF AG

Inventor： AMBERG WILHELM ,  JANSEN ROLF ,  KETTSCHAU GEORG ,  HERGENROEDER STEFAN ,  RASCHACK MANFRED ,  UNGER LILIANE

IPC: C07D251/22 ,  A61K31/505 ,  A61K31/517 ,  A61K31/519 ,  A61K31/53 ,  A61K45/00 ,  A61P9/04 ,  A61P9/10 ,  A61P9/12 ,  A61P13/08 ,  A61P13/12 ,  A61P35/00 ,  A61P43/00 ,  C07D239/34 ,  C07D239/52 ,  C07D239/60 ,  C07D239/70 ,  C07D251/52 ,  C07D401/12 ,  C07D403/12 ,  C07D405/12 ,  C07D491/048 ,  C07D495/04 ,  C07D ,  A61K

Abstract: The invention relates to new carboxylic acid derivatives of the formula (I), where the substituents have the meaning given in the description, their production and their use as endothelin-receptor antagonists.

公开(公告)号：BR0011105A

公开(公告)日：2002-03-05

申请号：BR0011105

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：NZ502319A

公开(公告)日：2002-03-01

申请号：NZ50231998

申请日：1998-06-05

Applicant: BASF AG

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

IPC: C07D251/16 ,  A61K31/4965 ,  A61K31/50 ,  A61K31/505 ,  A61K31/517 ,  A61K31/519 ,  A61K31/53 ,  A61P7/02 ,  A61P9/02 ,  A61P9/04 ,  A61P9/10 ,  A61P9/12 ,  A61P11/06 ,  A61P13/08 ,  A61P13/12 ,  A61P25/06 ,  A61P35/00 ,  A61P35/04 ,  A61P43/00 ,  C07C247/12 ,  C07D213/68 ,  C07D237/14 ,  C07D237/16 ,  C07D239/34 ,  C07D239/52 ,  C07D239/56 ,  C07D239/60 ,  C07D239/70 ,  C07D239/80 ,  C07D239/95 ,  C07D241/18 ,  C07D251/22 ,  C07D251/34 ,  C07D251/52 ,  C07D253/06 ,  C07D403/12 ,  C07D491/048 ,  C07C235/12 ,  C07C233/63 ,  C07C229/22 ,  C07C233/47 ,  C07C235/34

Abstract: An b-amino or b-azido carboxylic acid derivative has the formula (I) wherein: R1 is tetrazole or -C(=O)-R; R is OR4, -O-(CH2)p-S(O)k-R5, a 5 membered heteroaromatic system linked via a nitrogen atom, -NH-SO2-R5; A is NR7R8 or azido; W and Z are independently nitrogen or methine provided that Q is nitrogen if W and Z are methine; X is nitrogen or CR9; Y is nitrogen or CR10; Q is nitrogen or CR11 provided that if X is CR9 and Y is CR10 if Q is nitrogen; R2 and R3 are independently optionally substituted phenyl or naphthyl or phenyl or naphthyl is linked together in ortho position by a direct linkage, methylene, ethylene or ethenylene, oxygen, sulphur, SO2, NH or N-alkyl; R4 is H, alkali metal cation, alkaline earth metal cation, or a physiologically tolerated organic ammonium ion, optionally substituted cycloalkyl, alkyl or -CH2-phenyl. k is 0 to 2 and p is 1 to 4; R5 is alkyl, cycloalkyl, alkenyl, alkynyl or optionally substituted phenyl and R7 to R11 are defined in the specification. A pharmaceutical composition thereof is useful as an endothelin receptor antagonist. A compound of formula (II) A-C(R2)(R3)-CH(R1)-OH wherein A and R1 to R3 are as defined above s useful as a starting material to prepare the compounds of formula (I).

公开(公告)号：SI9520061B

公开(公告)日：2002-02-28

申请号：SI9520061

申请日：1995-04-26

Applicant: BASF AG

Inventor： AMBERG WILHELM ,  BERNARD HARALD ,  BUSCHMANN ERNST ,  HAUPT ANDREAS ,  JANITSCHKE LOTHAR ,  JANSSEN BERND ,  KARL ULRICH ,  KLING ANDREAS ,  MUELLER STEFAN ,  DE POTZOLLI BERND ,  RITTER KURT ,  THYES MARCO ,  ZIERKE THOMAS

IPC: A61K38/08 ,  A61K38/00 ,  A61P35/00 ,  C07K1/08 ,  C07K5/10 ,  C07K5/103 ,  C07K7/06 ,  C07K14/52

Abstract: PCT No. PCT/EP95/01577 Sec. 371 Date Nov. 4, 1996 Sec. 102(e) Date Nov. 4, 1996 PCT Filed Apr. 26, 1995 PCT Pub. No. WO95/30691 PCT Pub. Date Nov. 16, 1995The compound Me2Val-Val-MeVal-Pro-Pro-NHBzlxHCl is described. It is prepared from Z-Val-Val-MeVal-Pro-OR1 where Z and R1 have the meanings stated in the description. The compound shows antineoplastic activity.

公开(公告)号：HU0103560A2

公开(公告)日：2002-02-28

申请号：HU0103560

申请日：1999-06-23

Applicant: BASF AG

Inventor： AMBERG WILHELM ,  BARLOZZARI TERESA ,  HAUPT ANDREAS ,  JANSSEN BERND ,  KLING ANDREAS ,  RITTER KURT

IPC: A61K38/00 ,  A61K35/56 ,  A61P35/00 ,  C07K5/103 ,  C07K5/117 ,  C07K7/02

Abstract: Compounds of the present invention include cell growth inhibitors which are peptides of Formula IA-B-D-E-F-G(I)and acid salts thereof, wherein A, D, and E are alpha -amino acid residues, B is an alpha -amino acid residue or an alpha -hydroxy acid residue, F is an aminobenzoic acid residue or an aminocycloalkanecarboxylic acid residue, and G is a monovalent radical, such as, for example, a hydrogen atom, an amino group, an alkyl group, an alkylene alkyl ether, an alkylene alkyl thioether, an alkylene aldehyde, an alkylene amide, a beta -hydroxylamino group, a hydrazido group, an alkoxy group, a thioalkoxy group, an aminoxy group, an oximato group, an alkylene aryl group, an alkylene ester, an alkylene sulfoxide or an alkylene sulfone. Another aspect of the present invention includes pharmaceutical compositions comprising a compound of Formula I and a pharmaceutically acceptable carrier. An additional embodiment of the present invention is a method for treating cancer in a mammal, such as a human, comprising administering to the mammal an effective amount of a compound of Formula I in a pharmaceutically acceptable composition.