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：CA2177602C

公开(公告)日：2007-01-02

申请号：CA2177602

申请日：1994-11-26

Applicant: BASF AG

Inventor： MUNSCHAUER RAINER ,  UNGER LILIANE ,  STEINER GERD ,  TESCHENDORF HANS-JURGEN ,  HOGER THOMAS

IPC: C07D209/44 ,  A61K31/40 ,  A61K31/403 ,  A61K31/404 ,  A61K31/42 ,  A61P21/02 ,  A61P25/08 ,  A61P25/20 ,  A61P25/24 ,  A61P25/26 ,  C07D209/14 ,  C07D209/18 ,  C07D209/52 ,  C07D409/12 ,  C07D487/04 ,  C07D491/048 ,  C07D497/04 ,  C07D498/04

Abstract: Compounds of formula (I) where B, R1, R2, n and A have the meanings given in the description, and their preparation are described. The novel compounds ar e suitable for the control of diseases.

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：CA2241787C

公开(公告)日：2006-04-04

申请号：CA2241787

申请日：1997-01-10

Applicant: BASF AG

Inventor： TESCHENDORF HANS-JURGEN ,  WICKE KARSTEN ,  TREIBER HANS-JORG ,  STARCK DOROTHEA ,  BLANK STEFAN ,  UNGER LILIANE

IPC: C07D243/08 ,  C07D403/14 ,  A61K31/00 ,  A61K31/40 ,  A61K31/4025 ,  A61K31/41 ,  A61K31/44 ,  A61K31/4427 ,  A61K31/4433 ,  A61K31/4439 ,  A61K31/505 ,  A61K31/506 ,  A61K31/55 ,  A61K31/551 ,  A61K31/5513 ,  A61P25/18 ,  A61P43/00 ,  C07D213/73 ,  C07D223/04 ,  C07D245/02 ,  C07D401/04 ,  C07D401/14 ,  C07D403/02 ,  C07D403/04 ,  C07D403/06 ,  C07D403/10 ,  C07D403/12 ,  C07D405/14 ,  C07D409/12 ,  C07D409/14 ,  C07D413/14 ,  C07D417/06 ,  C07D417/12 ,  C07D417/14

Abstract: The present invention concerns aza- and diazacycloheptane and cyclooctane compounds from the following formula (I) Ar1-A-B-Ar2 wherein Ar1, A, B, and Ar2 have the meanings given in the description. The compounds according to the invention possess a high affinity with the dopamine-D3-receptors and can therefore be used for the treatment o f illness, which react to dopamine-D3-ligands.

公开(公告)号：CA2176962C

公开(公告)日：2005-12-20

申请号：CA2176962

申请日：1994-11-26

Applicant: BASF AG

Inventor： STEINER GERD ,  MUNSCHAUER RAINER ,  UNGER LILIANE ,  TESCHENDORF HANS-JURGEN ,  HOGER THOMAS

IPC: A61K31/395 ,  C07D209/44 ,  C07D403/00 ,  C07D405/00 ,  C07D409/00 ,  C07D413/00 ,  C07D417/00

Abstract: The invention pertains to compounds of formula (I) where the substituents are as indicated in the description, and to their preparation. The new compounds can be used to combat diseases.

公开(公告)号：CA2138287C

公开(公告)日：2005-03-01

申请号：CA2138287

申请日：1993-06-08

Applicant: BASF AG

Inventor： STEINER GERD ,  UNGER LILIANE ,  BEHL BERTHOLD ,  TESCHENDORF HANS-JUERGEN

IPC: C07D401/04 ,  A61K31/40 ,  A61K31/403 ,  A61K31/4427 ,  A61K31/4433 ,  A61K31/4439 ,  A61K31/445 ,  A61P25/00 ,  A61P25/02 ,  A61P25/20 ,  A61P43/00 ,  C07D209/52 ,  C07D409/04 ,  A61K31/44 ,  C07D403/04

Abstract: Compounds of the formula I: (See formula I) in which the substituents have the meanings stated in the description, and their preparation are described. These novel compounds are suitable as neuroleptics, antidepressants, sedatives, hypnotics, CNS protectives or muscle relaxants.

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.

公开(公告)号：HRP20010590A2

公开(公告)日：2003-08-31

申请号：HRP20010590

申请日：2001-08-10

Applicant: BASF AG

Inventor： STARCK DOROTHEA ,  TREIBER HANS-JOERG ,  UNGER LILIANE ,  NEUMANN-SCHULTZ BARBARA ,  BLUMBACH KAI ,  SCHOEBEL DIETMAR

IPC: C07D249/14 ,  A61K31/41 ,  A61K31/4196 ,  A61K31/422 ,  A61K31/4245 ,  A61K31/427 ,  A61K31/436 ,  A61K31/4439 ,  A61K31/4725 ,  A61K31/473 ,  A61K31/496 ,  A61K31/497 ,  A61K31/5377 ,  A61K31/55 ,  A61P3/04 ,  A61P9/00 ,  A61P9/10 ,  A61P13/12 ,  A61P15/10 ,  A61P25/00 ,  A61P25/08 ,  A61P25/14 ,  A61P25/16 ,  A61P25/18 ,  A61P25/20 ,  A61P25/22 ,  A61P25/28 ,  A61P25/30 ,  A61P25/32 ,  A61P25/34 ,  A61P25/36 ,  A61P43/00 ,  C07D249/12 ,  C07D401/04 ,  C07D401/06 ,  C07D401/12 ,  C07D401/14 ,  C07D403/04 ,  C07D403/06 ,  C07D403/12 ,  C07D403/14 ,  C07D405/06 ,  C07D405/14 ,  C07D409/04 ,  C07D409/14 ,  C07D413/14 ,  C07D417/04 ,  C07D417/12 ,  C07D417/14 ,  C07D491/04 ,  C07D491/052 ,  A61P25/24

Abstract: Triazole compounds of the following formulawhere R1, R2, A and B have the meanings given in the description are described. The compounds according to the invention possess a high affinity for the dopamine D3 receptor and can therefore be used for treating diseases which respond to the influence of dopamine D3 ligands.

公开(公告)号：DE59510596D1

公开(公告)日：2003-04-24

申请号：DE59510596

申请日：1995-07-14

Applicant: BASF AG

Inventor： HELLENDAHL BEATE ,  LANSKY ANNEGRET ,  RENDENBACH-MUELLER BEATRICE ,  BACH ALFRED ,  UNGER LILIANE ,  TESCHENDORF HANS-JUERGEN ,  WICKE KARSTEN

IPC: C07D277/22 ,  A61K31/425 ,  A61K31/426 ,  A61K31/433 ,  A61K31/435 ,  A61K31/44 ,  A61K31/4439 ,  A61K31/445 ,  A61K31/454 ,  A61K31/496 ,  A61K31/54 ,  C07D277/20 ,  C07D277/32 ,  C07D277/36 ,  C07D277/42 ,  C07D285/12 ,  C07D285/125 ,  C07D285/135 ,  C07D417/12

Abstract: PCT No. PCT/EP95/02783 Sec. 371 Date Jan. 14, 1997 Sec. 102(e) Date Jan. 14, 1997 PCT Filed Jul. 14, 1995 PCT Pub. No. WO96/02249 PCT Pub. Date Feb. 1, 1996The present invention relates to the use of thiazole and thiadiazole compounds of the following formula: where R1, A, B and Ar have the meanings stated in the description. The compounds according to the invention have a high affinity for the dopamine D3 receptor and can therefore be used to treat disorders of the central nervous system.