公开(公告)号：BG104400A

公开(公告)日：2001-01-31

申请号：BG10440000

申请日：2000-05-04

Applicant: BASF AG

Inventor： AMBERG WILHELM ,  JANSEN ROLF ,  HILLEN HEINZ ,  HERGENROEDER STEFAN ,  RASCHAK 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 invention relates to carboxylic acid derivatives of formula wherein A represents NR8R9, azido, OR10, SR10 or C1-C4 alkyl, R1 represents tetrazole or a group (1) wherein R has the following meaning: a) a radical OR5; b) a 5-membered heteroaromat bonded by a nitrogen atom; c) a group (2); d) a radical (3), and the remaining substituents have the meanings given in the description. The invention also relates to production of the inventive derivatives and to their use as endothelin receptor antagonists. 9 claims

公开(公告)号：DE19933164A1

公开(公告)日：2001-01-25

申请号：DE19933164

申请日：1999-07-20

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：CA2379545A1

公开(公告)日：2001-01-25

申请号：CA2379545

申请日：2000-07-05

Applicant: BASF AG

Inventor： KETTSCHAU GEORG ,  AMBERG WILHELM

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：NO20010046D0

公开(公告)日：2001-01-04

申请号：NO20010046

申请日：2001-01-04

Applicant: BASF AG ,  BASF BIORES CORP

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

IPC: A61K38/00 ,  A61K35/56 ,  A61P35/00 ,  C07K5/103 ,  C07K5/117 ,  C07K7/02 ,  C07K

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.

公开(公告)号：CO4990973A1

公开(公告)日：2000-12-26

申请号：CO98067231

申请日：1998-11-13

Applicant: BASF AG

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

IPC: C07D249/12 ,  A61K31/19 ,  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: Derivados del ácido a-hidroxicarboxílicoheterocíclicamente sustituido:en donde R1 significa tetrazol o un grupo:en donde R tiene el siguiente significado:a) un resto OR5 , en donde R5 significa:hidrógeno, el catión de un metal alcalino, el catión de un metal alcalinotérreo o un ion amonio orgánico fisiológicamente tolerable;cicloalquilo C3 -C8 , alquilo C1 -C8 , CH2 -fenilo, alquenilo C3 -C8 , alquinilo-C3 -C8 o fenilo eventualmente sustituidosb) un compuesto heteroaromático de 5 miembros, ligado a través de un átomo de nitrógeno.c) un grupo:en el cual k puede tomar los valores 0, 1 y 2, p los valores 1, 2, 3 y 4 y R6 representan alquilo C1 -C4 , cicloalquilo C3 -C8 , alquenilo C3 -C8 , alquinilo C3 -C8 o fenilo eventualmente sustituido.d) un resto:en donde R7 significa:alquilo-C1 -C4 , alquenilo-C3 -C8 , alquinilo-C3 - C8 , cicloalquilo-C3 -C8 , pudiendo estos restos llevar un resto alcoxi C1 -C4 , alquiltio C1 -C4 y/o un resto fenilo, ...

公开(公告)号：DE59606132D1

公开(公告)日：2000-12-14

申请号：DE59606132

申请日：1996-08-29

Applicant: BASF AG

Inventor： AMBERG WILHELM ,  KLING ANDREAS ,  KLINGE DAGMAR ,  RIECHERS HARTMUT ,  UNGER LILIANE ,  RASCHACK MANFRED ,  HERGENROEDER STEFAN ,  ELGER BERND ,  SCHULT SABINE

IPC: C07D317/02 ,  A61K31/00 ,  A61K31/19 ,  A61K31/192 ,  A61K31/34 ,  A61K31/341 ,  A61K31/343 ,  A61K31/35 ,  A61K31/352 ,  A61K31/357 ,  A61K31/36 ,  A61K31/435 ,  A61K31/44 ,  A61K31/505 ,  A61P9/00 ,  A61P9/08 ,  C07C53/134 ,  C07C57/30 ,  C07C57/32 ,  C07C57/38 ,  C07C59/64 ,  C07C69/616 ,  C07C69/734 ,  C07C255/00 ,  C07D213/55 ,  C07D213/64 ,  C07D221/04 ,  C07D239/26 ,  C07D239/34 ,  C07D239/52 ,  C07D239/70 ,  C07D257/04 ,  C07D307/79 ,  C07D317/50 ,  C07D317/60 ,  C07D319/02 ,  C07D319/18

Abstract: PCT No. PCT/EP96/03793 Sec. 371 Date Feb. 24, 1998 Sec. 102(e) Date Feb. 24, 1998 PCT Filed Aug. 29, 1996 PCT Pub. No. WO97/09294 PCT Pub. Date Mar. 13, 1997Carboxylic acid derivatives of the formula I here R1 is a tetrazole [sic], nitrile [sic], a group COOH or a radical which can be hydrolyzed to COOH, and the other substituents have the meaning explained in the description.

公开(公告)号：ZA991779B

公开(公告)日：2000-10-11

申请号：ZA991779

申请日：1999-03-05

Applicant: BASF AG

Inventor： AMBERG WILHELM ,  KLINGE ROLF JANSEN DAGMAR

IPC: A61K31/19 ,  A61K31/215 ,  A61K31/357 ,  C07D239/38 ,  A61K31/36 ,  A61K31/505 ,  A61P43/00 ,  C07C319/14 ,  C07C323/56 ,  C07D239/56 ,  C07D239/60 ,  C07D317/62 ,  C07D ,  C07B ,  C07C

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：ZA9901738B

公开(公告)日：2000-10-11

申请号：ZA9901738

申请日：1999-03-04

Applicant: BASF AG

Inventor： AMBERG WILHELM ,  KLINGE ROLF JANSEN DAGMAR ,  RIECHERS HARTMUT ,  HERGENROEDER 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 ,  C07D ,  A61K

CPC classification number: C07D239/52 ,  C07C59/68 ,  C07C69/734 ,  C07D239/34

公开(公告)号：NO20004351L

公开(公告)日：2000-09-01

申请号：NO20004351

申请日：2000-09-01

Applicant: BASF AG

Inventor： AMBERG WILHELM ,  JANSEN ROLF ,  KLINGE DAGMAR ,  RIECHERS HARTMUT ,  HERGENROEDER 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

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：HRP950271B1

公开(公告)日：2000-08-31

申请号：HRP950271

申请日：1995-05-04

Applicant: BASF AG

Inventor： AMBERG WILHELM ,  HARALD BERNARD ,  BUSCHMANN ERNST ,  HAUPT ANDREAS ,  JANITSCHKE LOTHAR ,  JANSSEN BERND ,  KARL ULRICH ,  KLING ANDREAS ,  MULLER STEFAN ,  POTZOLLI BERND DE ,  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.