公开(公告)号：WO0190079A3

公开(公告)日：2002-04-04

申请号：PCT/EP0105742

申请日：2001-05-18

Applicant: BASF AG ,  AMBERG WILHELM ,  KETTSCHAU GEORG

Inventor： AMBERG WILHELM ,  KETTSCHAU GEORG

IPC: C07D251/22 ,  A61K31/44 ,  A61K31/505 ,  A61K31/506 ,  A61K31/519 ,  A61K31/53 ,  A61K31/5377 ,  A61P1/18 ,  A61P7/10 ,  A61P9/00 ,  A61P9/04 ,  A61P9/10 ,  A61P9/12 ,  A61P13/08 ,  A61P13/12 ,  A61P15/10 ,  A61P43/00 ,  C07D213/69 ,  C07D239/34 ,  C07D239/52 ,  C07D239/60 ,  C07D239/70 ,  C07D241/18 ,  C07D401/12 ,  C07D403/12 ,  C07D491/048 ,  C07D495/04

CPC classification number: C07D239/60 ,  C07D239/34

Abstract: The invention relates to carbamate and carbamide derivatives of formula (I), wherein the substituents have the meaning cited in the description. The invention also relates to the production and use thereof as endothelin receptor antagonists.

Abstract translation: 本发明涉及其中取代基在说明书所说明的式（I），以及它们的制备氨基甲酸酯和脲衍生物和作为内皮素受体拮抗剂使用。

公开(公告)号：WO0073276A3

公开(公告)日：2001-05-10

申请号：PCT/EP0004571

申请日：2000-05-19

Applicant: BASF AG ,  AMBERG WILHELM ,  KETTSCHAU GEORG

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

CPC classification number: C07D251/30 ,  A61K31/505 ,  A61K31/517 ,  A61K31/519 ,  A61K31/53 ,  C07D239/34 ,  C07D239/52

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.

Abstract translation: 本发明涉及羧酸的式（I）其中取代基是在说明书，制备如所解释和作为内皮素受体拮抗剂使用的衍生物。

公开(公告)号：WO9722621A3

公开(公告)日：1998-02-26

申请号：PCT/EP9605518

申请日：1996-12-11

Applicant: BASF AG ,  AMBERG WILHELM ,  BARLOZZARI TERESA ,  BERNARD HARALD ,  BUSCHMANN ERNST ,  HAUPT ANDREAS ,  HEGE HANS GUENTHER ,  JANSSEN BERND ,  KLING ANDREAS ,  LIETZ HELMUT ,  RITTER KURT ,  ULLRICH MARTINA ,  WEYMANN JUERGEN ,  ZIERKE THOMAS

Inventor： AMBERG WILHELM ,  BARLOZZARI TERESA ,  BERNARD HARALD ,  BUSCHMANN ERNST ,  HAUPT ANDREAS ,  HEGE HANS-GUENTHER ,  JANSSEN BERND ,  KLING ANDREAS ,  LIETZ HELMUT ,  RITTER KURT ,  ULLRICH MARTINA ,  WEYMANN JUERGEN ,  ZIERKE THOMAS

IPC: A61K38/00 ,  A61K31/00 ,  A61K38/08 ,  A61P35/00 ,  A61P35/02 ,  C07K1/00 ,  C07K7/06

CPC classification number: A61K38/08

Abstract: Novel peptides of the following formula (I): R1R2N-CHX-CO-A-B-D-E-(G)¿s?-K in which R?1, R2¿, A, B, D, E, G, K, X, and s have the meanings stated in the description, and the preparation thereof are described. The novel peptides have an antineoplastic effect.

公开(公告)号：WO0124827A3

公开(公告)日：2002-05-10

申请号：PCT/EP0009671

申请日：2000-10-02

Applicant: BASF AG ,  AMBERG WILHELM ,  KLING ANDREAS ,  HORNBERGER WILFRIED

Inventor： AMBERG WILHELM ,  KLING ANDREAS ,  HORNBERGER WILFRIED

IPC: A61K38/00 ,  A61K45/00 ,  A61K45/06 ,  A61P9/00 ,  A61P9/08 ,  A61P9/10 ,  A61P19/02 ,  A61P29/00 ,  A61P37/06 ,  A61P43/00 ,  C07D239/34 ,  C07D263/34 ,  C07D277/48 ,  C07D307/68 ,  C07D333/38 ,  C07D401/04 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D403/14 ,  C07D405/04 ,  C07D405/14 ,  C07D409/12 ,  C07D409/14 ,  C07D413/12 ,  C07D417/12 ,  C07D417/14 ,  C07K5/02

CPC classification number: C07D263/34 ,  A61K38/00 ,  A61K45/06 ,  C07D239/34 ,  C07D277/48 ,  C07D307/68 ,  C07D333/38 ,  C07D401/04 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D403/14 ,  C07D405/04 ,  C07D405/14 ,  C07D409/12 ,  C07D409/14 ,  C07D413/12 ,  C07D417/12 ,  C07D417/14 ,  C07K5/0202

Abstract: The invention relates to the use of an endothelin blocker in combination with an alpha v beta 3 integrin receptor antagonist for the treatment or prevention of diseases, particularly to the use of a pharmaceutical composition, comprising an endothelin blocker and an alpha v beta 3 integrin receptor antagonist, for the treatment or prevention of cardiovascular disorders, particularly for the treatment or prevention of restenosis after vessel injury or revascularisation treatment and to the pharmaceutical composition itself.

Abstract translation: 本发明涉及内皮素阻滞剂与αvβ3整联蛋白受体拮抗剂组合用于治疗或预防疾病，特别是包含内皮素阻断剂和αvβ3整联蛋白受体的药物组合物的使用 拮抗剂，用于治疗或预防心血管疾病，特别是用于治疗或预防血管损伤或血运重建治疗后的再狭窄以及药物组合物本身。

公开(公告)号：WO9944988A3

公开(公告)日：1999-11-11

申请号：PCT/EP9901209

申请日：1999-02-25

Applicant: BASF AG ,  AMBERG WILHELM ,  JANSEN ROLF ,  KLINGE DAGMAR

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

CPC classification number: C07C319/14 ,  C07D239/60

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.

Abstract translation: 一种通式（I）Sulfanyltyp的内皮素受体拮抗剂，其中，R <1>是羟基，烷氧基，sulfonamidyl，氨基的制备方法中，R <2>是烷基，芳基或杂芳基，任选被取代，且R <3>，R <4> ，R <5>相同或独立地为烷基或芳基，任选被取代的，可通过用下式的硫化物式（II）的羧酸衍生物的亲核反应而制备（III），其中X为SR <6>或SO 2 <6>，和 [R <6>是烷基或芳基可任选被取代，式（I）的内皮素受体拮抗剂。

公开(公告)号：WO9809953A3

公开(公告)日：1998-10-29

申请号：PCT/EP9704688

申请日：1997-09-02

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

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

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

Abstract: Carboxylic acid derivatives have the formula (I), in which R1 stands for tetrazole or a group (a); R2 stands for hydrogen, hydroxy, NH¿2?, NH(C1-c4-alkyl), N(C1-C4-alkyl)2, halogen, C1-C4-alkyl, C2-C4-alkenyl, C2-C4-alkinyl, C1-C4-halogenalkyl, C1-C4-alkoxy, C1-C4-halogenalkoxy or C1-C4-alkylthio, or CR?2¿ is linked with CR10, as indicated below, into a 5- or 6-membered ring; X stands for nitrogen or methine; Y stands for nitrogen or methine; Z stands for nitrogen or CR10, wherein R10 is hydrogen or C¿1?-C4-alkyl or CR?10¿ forms together with CR?2 or CR3¿ an optionally substituted 5- or 6-membered alkylene or alkenylene ring, and wherein one or more methylene groups can be substituted by oxygen, sulphur, -NH or -N(C¿1?-C4-alkyl); R?3¿ stands for hydrogen, hydroxy, NH¿2?, NH(C1-C4-alkyl), N(C1-C4-alkyl)2, halogen, C1-C4-alkyl, C2-C4-alkenyl, C2-C4-alkinyl, C1-C4-hydroxyalkyl, C1-C4-halogenalkyl, C1-C4-alkoxy, C1-C4-halogenalkoxy, C1-C4-alkylthio; or CR?3¿ is linked to CR10 as indicated above into a 5- or 6-membered ring, R?4 and R5¿ (which may be identical or different) stand for optionally substituted phenyl or naphthyl, or for phenyl or naphthyl which are linked to each other at the ortho-position by a direct bond, a methylene, ethylene or ethenylene group, an oxygen or sulphur atom or an SO¿2?, NH or N-alkyl group; optionally substituted C3-C8-cycloalkyl; R?6¿ stands for optionally substituted C¿3?-C8-cycloalkyl; optionally substituted phenyl or naphthyl, a 5- or 6-membered, optionally substituted heteroaromatic compound containing one to three nitrogen atoms and/or one sulphur or oxygen atom; W stands for sulphur or oxygen; Q is a spacer with a length that corresponds to a C2-C4 chain. Also disclosed are the physiologically tolerable salts of these compounds, as well as their pure enantiomer and diastereoisomer forms, their preparation and use as mixed ETA/ETB-receptor antagonists.

公开(公告)号：WO9923078A3

公开(公告)日：1999-09-10

申请号：PCT/EP9806571

申请日：1998-10-16

Applicant: BASF AG ,  AMBERG WILHELM ,  JANSEN ROLF ,  HERGENROEDER STEFAN ,  RASCHACK MANFRED ,  UNGER LILIANE

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

CPC classification number: C07D239/36 ,  C07D239/52 ,  C07D239/60 ,  C07D401/12

Abstract: The invention relates to carboxylic acid derivatives of formula (I), wherein R represents a group (a) or (b), R and R being the same or different and having the following meaning: hydrogen; on the condition that R and R are not hydrogen at the same time, C1-C8-alkyl, C3-C8-cycloalkyl, C3-C8-alkenyl, C3-C8-alkinyl, benzyl, phenyl, naphthyl, optionally substituted; or R and R together form an optionally substituted C3-C7-alkylene chain which is closed in a ring and in which an alkylene group can be replaced by oxygen, sulphur or nitrogen; or R and R together form an optionally substituted C3-7-alkylene chain or C3-C7-alkenylene chain which is closed in a ring and to which an optionally substituted phenyl ring is anellated. The other substituents have the meanings given in the description. The invention also relates to the production of the novel carboxylic acid derivatives and to their use as endothelin receptor antagonists.

Abstract translation: 本发明涉及式（I）式的羧酸衍生物，其中R <6>是基团（a）或（b）具有R <13>和R <14>可以相同或不同，且定义如下; 前提氢是R <13>和R <14>决不能同时为氢，C1-C8烷基，C3-C8环烷基，C3-C8链烯基，C3-C8炔基，苄基，苯基，萘基 中，每个任选地被取代，或R <13>和R <14>一起形成，以形成闭环，其中的亚烷基可以被氧，硫或氮，或者R来代替任选取代的C3-C7亚烷基链<13> 且R <14>一起形成环的闭合，任选取代的C 3 -C 7 - 亚烷基或C 3 -C 7 - 亚烯基链，其中苯基环稠合任选被取代; 并且其中，所述其它取代基是在说明书，用作内皮素受体拮抗剂的制备所述的相同。

公开(公告)号：CA2223911C

公开(公告)日：2009-03-24

申请号：CA2223911

申请日：1996-07-12

Applicant: BASF AG

Inventor： HAUPT ANDREAS ,  JANSSEN BERND ,  KARL ULRICH ,  KLING ANDREAS ,  ZIERKE THOMAS ,  MULLER STEFAN ,  RITTER KURT ,  BUSCHMANN ERNST ,  AMBERG WILHELM ,  BERNARD HARALD

IPC: C07K1/02 ,  C07K11/00 ,  C07K1/12 ,  C07K5/06 ,  C07K5/078 ,  C07K5/08 ,  C07K5/083 ,  C07K5/10 ,  C07K5/103 ,  C07K7/06 ,  C12P21/02

Abstract: The description relates to a process for producing pentapeptides of the formula (I) in which A and R1-R3 have the meanings given, in which the pentapeptide is constructed in steps from a prolinamide of the formula (II) in which R1 and R2 have the meanings given above, and the group -NR1R2 may be hydrolytically separated from the peptide thus obtained.

公开(公告)号：CA2201785C

公开(公告)日：2006-08-29

申请号：CA2201785

申请日：1995-10-07

Applicant: BASF AG

Inventor： VOGELBACHER UWE JOSEF ,  KLING ANDREAS ,  MULLER STEFAN ,  BAUMANN ERNST ,  RHEINHEIMER JOACHIM ,  KLINGE DAGMAR ,  AMBERG WILHELM ,  RIECHERS HARTMUT ,  UNGER LILIANE ,  WERNET WOLFGANG ,  RASCHACK MANFRED

IPC: C07D239/28 ,  C07D251/30 ,  A61K31/505 ,  A61K31/506 ,  A61P9/00 ,  A61P9/08 ,  A61P9/10 ,  A61P9/12 ,  A61P11/08 ,  A61P13/02 ,  A61P15/00 ,  A61P25/04 ,  C07D239/00 ,  C07D239/26 ,  C07D239/34 ,  C07D239/38 ,  C07D239/60 ,  C07D239/70 ,  C07D239/96 ,  C07D251/12 ,  C07D251/52 ,  C07D257/02 ,  C07D309/00 ,  C07D403/06 ,  C07D403/12 ,  C07D405/12 ,  C07D417/12 ,  C07D487/04 ,  C07D491/04 ,  C07D491/044 ,  C07D491/048

Abstract: Carboxylic acid derivatives have the formula (I), in which R to R6, X, Y, and Z have the meanings given in the description. Also disclosed is their preparation. These new compounds are useful for controlling diseases.

公开(公告)号：HRP950517B1

公开(公告)日：2004-06-30

申请号：HRP950517

申请日：1995-10-13

Applicant: BASF AG

Inventor： RIECHERS HARTMUT ,  KLINGE DAGMAR ,  AMBERG WILHELM ,  KLING ANDREAS ,  MUELLER STEFAN ,  BAUMANN ERNST ,  RHEINHEIMER JOACHIM ,  VOGELBACHER UWE JOSEF ,  WERNET WOLFGANG ,  UNGER LILIANE ,  RASCHACK MANFRED

IPC: C07D251/30 ,  A61K31/505 ,  A61P9/00 ,  A61P9/08 ,  A61P9/10 ,  A61P9/12 ,  A61P11/08 ,  A61P13/02 ,  A61P15/00 ,  A61P25/04 ,  C07D239/00 ,  C07D239/26 ,  C07D239/28 ,  C07D239/34 ,  C07D239/38 ,  C07D239/60 ,  C07D239/70 ,  C07D239/96 ,  C07D251/12 ,  C07D251/52 ,  C07D257/02 ,  C07D309/00 ,  C07D403/06 ,  C07D403/12 ,  C07D405/12 ,  C07D417/12 ,  C07D487/04 ,  C07D491/04 ,  C07D491/044 ,  C07D491/048

Abstract: Heterocyclyl-substd. propanoic acids and their derivs., of formula (I), are new. R = formyl, tetrazolyl, nitrile, COOH or a gp. that can be hydrolysed to COOH; X = N or CR14; R2 = H, OH, NH2, alkylamino, dialkylamino, halo, alkyl, haloalkyl, alkoxy, haloalkoxy or alkylthio; R14 = H or 1-5 C alkyl; R3 = R2 or alkoxyimino; or CR3 + CR14 = 5 or 6 membered alkylene or alkenyl ring (opt. substd. by 1-2 alkyl) in which a methylene can be replaced by O, S, NH or alkylamino; R4, R5 = phenyl or naphthyl (both opt. substd. by one or more halo, NO2, CN, OH, alkyl, haloalkyl, alkoxy, haloalkyloxy, phenoxy, alkylthio, NH2, alkylamine or dialkylamino) or 3-7 C cycloalkyl; or the phenyl or naphthyl gps. are opt. bonded at the O- position (by a bond, CH2, O, S, SO2, ethylene, ethenylene or opt. alkylated amino); R6 = H, 1-8 C alkyl, 2-6 C alkenyl, 3-6 C alkynyl, 3-8 C cycloalkyl (all opt. substd. by 1 or more halo, NO2, CN, alkoxy 3-6 C alkenyloxy, 3-6 C alkynyloxy, alkylthio, haloalkoxy, alkylcarbonyl, alkoxycarbonyl, 3-8 C alkylcarbonylalkyl, alkylamino, dialkylamino, phenyl, Ph or OPh), Ar or Het; Y = S, O or bond; Q = S, O, SO, SO2 or bond; Ph = substd. phenyl, where substits. are halo, NO2, CN, alkyl, haloalkyl, alkoxy, haloalkoxy or alkylthio; Ar = phenyl or naphthyl (both opt. substd. by 1 or more halo, NO2, CN, OH, NH2, alkylamino, dialkylamino or OCH2CH2O); Het = 5 or 6 membered heteroaromatic with 1-3 N atoms and/or one S or O (opt. substd. by 1-4 halo and/or 1 or 2 alkyl, haloalkyl, alkoxy, haloalkoxy, alkylthio, phenyl, phenoxy or phenyl carbonyl (where the phenyl is opt. substd. by 1-5 halo and/or 1-3 alkyl, haloalkyl, alkoxy, haloalkoxy and/or alkylthio)); alkyl and alkoxy have 1-4 C unless otherwise stated; provided that R6 is not H when Q = bond.