公开(公告)号：WO1997012878A1

公开(公告)日：1997-04-10

申请号：PCT/EP1996004205

申请日：1996-09-26

Applicant: BASF AKTIENGESELLSCHAFT ,  KLINGE, Dagmar ,  AMBERG, Wilhelm ,  KLING, Andreas ,  RIECHERS, Hartmut ,  UNGER, Liliane ,  RASCHACK, Manfred

Inventor： BASF AKTIENGESELLSCHAFT

IPC: C07D239/52

CPC classification number: C07D213/74 ,  C07D239/42 ,  C07D239/47 ,  C07D239/52 ,  C07D239/58 ,  C07D251/46

Abstract: The invention relates to amino acid derivatives of formula (I), in which the groups have the meaning given in the description. It also relates to the use thereof as inhibitors for endothelin receptors.

Abstract translation: 本发明涉及的氨基（I），其中的基团具有在说明书中给出的含义，下式的酸衍生物和它们作为内皮素受体抑制剂的用途。

公开(公告)号：WO1996011914A1

公开(公告)日：1996-04-25

申请号：PCT/EP1995003963

申请日：1995-10-07

Applicant: BASF AKTIENGESELLSCHAFT ,  RIECHERS, Hartmut ,  KLINGE, Dagmar ,  AMBERG, Wilhelm ,  KLING, Andreas ,  MÜLLER, Stefan ,  BAUMANN, Ernst ,  RHEINHEIMER, Joachim ,  VOGELBACHER, Uwe, Josef ,  WERNET, Wolfgang ,  UNGER, Liliane ,  RASCHACK, Manfred

Inventor： BASF AKTIENGESELLSCHAFT

IPC: C07D239/60

CPC classification number: C07D495/04 ,  C07D239/34 ,  C07D239/48 ,  C07D239/52 ,  C07D239/60 ,  C07D239/70 ,  C07D239/96 ,  C07D251/20 ,  C07D251/26 ,  C07D251/52 ,  C07D403/06 ,  C07D403/12 ,  C07D405/12 ,  C07D405/14 ,  C07D413/12 ,  C07D417/12 ,  C07D487/04 ,  C07D491/04 ,  C07D491/048

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

Abstract translation: 是式（I），其中R-R <6>，X，Y和Z具有在说明书中给出的含义，并且它们的生产的羧酸衍生物。 的新的化合物适于防治疾病。

公开(公告)号：WO1995030691A1

公开(公告)日：1995-11-16

申请号：PCT/EP1995001577

申请日：1995-04-26

Applicant: BASF AKTIENGESELLSCHAFT ,  AMBERG, Wilhelm ,  BERNARD, Harald ,  BUSCHMANN, Ernst ,  HAUPT, Andreas ,  JANITSCHKE, Lothar ,  JANSSEN, Bernd ,  KARL, Ulrich ,  KLING, Andreas ,  MÜLLER, Stefan ,  DE POTZOLLI, Bernd ,  RITTER, Kurt ,  THYES, Marco ,  ZIERKE, Thomas

Inventor： BASF AKTIENGESELLSCHAFT

IPC: C07K07/06

CPC classification number: C07K7/06 ,  A61K38/00 ,  C07K5/101 ,  Y02P20/55

Abstract: Disclosed is the compound Me2Val-Val-MeVal-Pro-Pro-NHBzl. HCl. The compound is produced from Z-Val-Val-MeVal-Pro-OR , wherein Z and R have the meanings indicated in the description. The compound disclosed has anti-neoplastic properties.

Abstract translation: 它是连接Me2Val-VAL -Meval-PRO-PRO-NHBz1。 HC1描述。 它是由Z-VAL-缬氨酸-Meval-PRO-OR <1>，其中Z和R <1>具有说明书中给出的含义的。 所述化合物具有抗肿瘤活性。

公开(公告)号：WO2007022964A3

公开(公告)日：2007-05-31

申请号：PCT/EP2006008279

申请日：2006-08-23

Applicant: ABBOTT GMBH & CO KG ,  AMBERG WILHELM ,  NETZ ASTRID ,  KLING ANDREAS ,  OCHSE MICHAEL ,  LANGE UDO ,  HUTCHINS CHARLES W ,  GARCIA-LADONA FRANCISCO JAVIER ,  WERNET WOLFGANG

Inventor： AMBERG WILHELM ,  NETZ ASTRID ,  KLING ANDREAS ,  OCHSE MICHAEL ,  LANGE UDO ,  HUTCHINS CHARLES W ,  GARCIA-LADONA FRANCISCO JAVIER ,  WERNET WOLFGANG

IPC: C07D213/75 ,  A61K31/44 ,  A61K31/4436 ,  A61K31/47 ,  A61K31/505 ,  A61P25/00 ,  C07D213/84 ,  C07D213/85 ,  C07D215/38 ,  C07D217/22 ,  C07D239/42 ,  C07D409/04

CPC classification number: C07D213/75 ,  A61K31/44 ,  A61K31/47 ,  A61K31/505 ,  C07D213/84 ,  C07D213/85 ,  C07D215/38 ,  C07D217/22 ,  C07D239/42 ,  C07D409/04

Abstract: The invention relates to the hetaryl-substituted guanidine compounds of general formula (I), enantiomeres, diastereomeres and/or tautomeres thereof, in addition to the pharmaceutically acceptable salts thereof and the prodrugs of the known compounds. The invention also relates to the use of said hetaryl-substituted guanidine compounds as binding partners for 5-HT5-receptors for treating and/or for the prophylaxis of illnesses which are modulated by a 5-HT5-receptor activity, in particular, for treating and/or for the prophylaxis of neurodegenerative and neuropsychiatric disorders, and signs, symptoms and dysfunctions associated with said disorders.

Abstract translation: 本发明涉及通式（I）的杂芳基 - 取代的胍化合物，对映体，非对映体和/或互变异构形式，以及它们的药学上可接受的盐，和所述的前药化合物。 此外，本发明化合物涉及使用杂芳基 - 取代的胍，作为对5-HT5受体，它们由5 HT5受体活性调节的疾病的治疗和/或预防的结合配偶体，特别是用于神经变性的治疗和/或预防和 神经精神障碍和相关体征，症状和功能障碍。

公开(公告)号：WO2007022946A1

公开(公告)日：2007-03-01

申请号：PCT/EP2006/008222

申请日：2006-08-21

Applicant: ABBOTT GMBH & CO. KG ,  AMBERG, Wilhelm ,  NETZ, Astrid ,  KLING, Andreas ,  OCHSE, Michael ,  LANGE, Udo ,  HUTCHINS, Charles, W. ,  GARCIA-LADONA, Francisco, Javier ,  WERNET, Wolfgang

Inventor： AMBERG, Wilhelm ,  NETZ, Astrid ,  KLING, Andreas ,  OCHSE, Michael ,  LANGE, Udo ,  HUTCHINS, Charles, W. ,  GARCIA-LADONA, Francisco, Javier ,  WERNET, Wolfgang

IPC: C07D215/38 ,  C07D239/84 ,  C07D401/12 ,  C07D409/12 ,  C07D471/04 ,  C07D493/04 ,  A61K31/498 ,  A61K31/4741 ,  A61K31/4709 ,  A61K31/4375 ,  A61K31/5377 ,  A61P25/00

CPC classification number: C07D491/056 ,  C07D215/38 ,  C07D239/84 ,  C07D401/04 ,  C07D401/12 ,  C07D405/06 ,  C07D409/04 ,  C07D409/12 ,  C07D471/04 ,  C07D491/04

Abstract: Die vorliegende Erfindung betrifft Verbindungen der allgemeinen Formel (I), entsprechende enantiomere, diastereomere und/oder tautomere Formen davon sowie pharmazeutisch annehmbare Salze davon sowie die Prodrugs der genannten Verbindungen. Weiterhin betrifft die vorliegende Verbindung die Verwendung der genannten Verbindungen als Bindungspartner für 5-HT5-Rezeptoren zur Behandlung von Krankheiten, die durch eine 5-HT5-Rezeptoraktivität moduliert werden, insbesondere zur Behandlung von neu rodegenerativen und neuropsychiatrischen Störungen sowie den damit zusammenhängenden Anzeichen, Symptomen und Fehlfunktionen.

Abstract translation: 本发明涉及通式（I），对映异构体对应，非对映体和/或互变异构形式的化合物，以及它们的化合物的前药，所述与药学上可接受的盐。 此外，本发明化合物涉及使用所述化合物作为5-HT5受体，它们通过5-HT5受体活性调节的，特别是用于神经变性和神经精神病症的治疗的疾病的治疗的结合配偶体，以及相关的征兆，症状 和故障。

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：WO1997038982A1

公开(公告)日：1997-10-23

申请号：PCT/EP1997001687

申请日：1997-04-04

Applicant: BASF AKTIENGESELLSCHAFT ,  AMBERG, Wilhelm ,  KLING, Andreas ,  KLINGE, Dagmar ,  RIECHERS, Hartmut ,  BAUMANN, Ernst ,  UNGER, Liliane ,  RASCHACK, Manfred ,  HERGENRÖDER, Stefan ,  SCHULT, Sabine

Inventor： BASF AKTIENGESELLSCHAFT

IPC: C07D239/60

CPC classification number: C07D215/227 ,  C07D239/34 ,  C07D239/60

Abstract: The present invention relates to carboxylic acid derivatives of formula (I) in which the radicals have the meaning given in the description, and the production of these substances and their use as medicaments.

Abstract translation: 本发明涉及式（I）式的羧酸衍生物，其中的基团具有在说明书中给出的含义，以及这些协议的制备方法以及它们作为药物的用途。

公开(公告)号：WO1997009294A1

公开(公告)日：1997-03-13

申请号：PCT/EP1996003793

申请日：1996-08-29

Applicant: BASF AKTIENGESELLSCHAFT ,  AMBERG, Wilhelm ,  KLING, Andreas ,  KLINGE, Dagmar ,  RIECHERS, Hartmut ,  UNGER, Liliane ,  RASCHACK, Manfred ,  HERGENRÖDER, Stefan ,  ELGER, Bernd ,  SCHULT, Sabine

Inventor： BASF AKTIENGESELLSCHAFT

IPC: C07C59/64

CPC classification number: C07D213/64 ,  C07C57/30 ,  C07C57/38 ,  C07C59/64 ,  C07C69/616 ,  C07C69/734 ,  C07D213/55 ,  C07D221/04 ,  C07D239/26 ,  C07D239/34 ,  C07D239/52 ,  C07D239/70 ,  C07D307/79 ,  C07D317/60 ,  C07D319/18

Abstract: Described are carboxylic acid derivatives of formula (I) in which R is a tetrazole or nitrile group, a COOH group or a group which can be hydrolysed to COOH, and the other substituents are as defined in the description.

Abstract translation: 式（I），其中R <1>表示四唑，腈，基团COOH或可水解与COOH基团且剩余取代基在说明书所解释的羧酸衍生物。