公开(公告)号：CZ9701132A3

公开(公告)日：1998-03-18

申请号：CZ113297

申请日：1995-10-07

Applicant: BASF AG

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

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 ,  A61K31/495

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

公开(公告)号：DE19614533A1

公开(公告)日：1997-10-16

申请号：DE19614533

申请日：1996-04-12

Applicant: BASF AG

Inventor： KLINGE DAGMAR DR ,  AMBERG WILHELM DR ,  BAUMANN ERNST DR ,  KLING ANDREAS DR ,  RIECHERS HARTMUT DR ,  UNGER LILIANE DR ,  RASCHACK MANFRED DR ,  HERGENROEDER STEFAN ,  SCHULT SABINE DR

IPC: A61K31/00 ,  A61K31/505 ,  A61K31/517 ,  A61P5/42 ,  A61P9/10 ,  A61P13/00 ,  A61P13/12 ,  C07D217/22 ,  C07D239/34 ,  C07D239/48 ,  C07D239/52 ,  C07D239/56 ,  C07D239/60 ,  C07D239/70 ,  C07D239/80 ,  C07D239/96 ,  C07D251/20 ,  C07D251/22 ,  C07D251/30 ,  C07D251/38 ,  C07D251/52 ,  C07D403/12 ,  C07D405/12 ,  C07D471/04 ,  C07D487/04 ,  C07D491/04 ,  C07D491/044 ,  C07D239/32 ,  A61K31/53 ,  A61K31/44 ,  A61K31/47

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

公开(公告)号：CZ9602873A3

公开(公告)日：1997-04-16

申请号：CZ287396

申请日：1995-03-23

Applicant: BASF AG

Inventor： BAUMANN ERNST DR ,  VOGELBACHER UWE JOSEF DR ,  RHEINHEIMER JOACHIM DR ,  KLINGE DAGMAR DR ,  RIECHERS HARTMUT DR ,  KROGER BURKHARD DR ,  BIALOJAN SIEGFRIED DR ,  BOLLSCHWEILER CLAUS DR ,  WERNER VOLFGANG DR ,  UNGER LILIANE DR ,  RASCHACK MANFRED DR

IPC: C07D251/26 ,  A61K31/505 ,  A61K31/506 ,  A61K31/53 ,  A61P9/00 ,  A61P9/08 ,  A61P9/10 ,  A61P9/12 ,  A61P11/08 ,  A61P13/02 ,  A61P15/00 ,  A61P25/04 ,  A61P39/02 ,  C07D239/26 ,  C07D239/34 ,  C07D239/38 ,  C07D401/12 ,  C07D405/12 ,  C07D409/12 ,  C07D413/12 ,  C07D417/12 ,  A61K31/00

CPC classification number: A61K31/505 ,  A61K31/506 ,  A61K31/53

公开(公告)号：DE4341663A1

公开(公告)日：1995-06-08

申请号：DE4341663

申请日：1993-12-07

Applicant: BASF AG

Inventor： UNGER LILIANE DR ,  RASCHACK MANFRED DR ,  WERNET WOLFGANG DR ,  BOEHM HANS-JOACHIM DR ,  RIECHERS HARTMUT DR

IPC: C07C205/26 ,  C07C205/37 ,  C07D241/44 ,  C07D401/06 ,  C07D403/06 ,  C07D241/52 ,  C07D487/04

Abstract: Bicyclic piperazinone derivs. of formula (I) and their salts are new. Two of A, B, D and E are CH and the other two are CH or N; G = 1-6C alkyl, (CH2)nG', COR1 or SO2R1; n = 0-4; G' = phenyl (opt. mono- or disubstd. by OH, 1-4C alkyl, 1-4C alkoxy, halogen or CF3), heteroaryl (opt. monosubstd. by OH, 1-4C alkyl, 1-4C alkoxy, halogen or CF3) or 3-6C cycloalkyl (opt. substd. by 1-3C alkyl); R1 = H or 1-6C alkyl; M, Q = a direct bond, 1-6C n-alkylene (opt. substd. by 1-6C alkyl or Ar) or CH=CH; Ar = phenyl (opt. mono- or disubstd. by OH, 1-4C alkyl, 1-4C alkoxy, halogen or CF3) or heteroaryl (opt. monosubstd. by OH, 1-4C alkyl, 1-4C alkoxy, halogen or CF3); L, T = COOR3, CONR3R4 or SO2OR3; R3 and R4 = H, 1-6C alkyl, OR5 or SR5; R5 = 1-6C alkyl or Ar; X, Y = H, 1-6C alkyl, 1-6C alkoxy or 1-6C alkylthio, phenyl or benzyl (both opt. mono- or disubstd. by OH, 1-4C alkyl, 1-4C alkoxy, halogen or CF3) or CONR3R4 or SO2NR3R4.

公开(公告)号：DE4308078A1

公开(公告)日：1994-09-15

申请号：DE4308078

申请日：1993-03-13

Applicant: BASF AG

Inventor： RIECHERS HARTMUT DR ,  ADAM GEO DR ,  MUENTER KLAUS DR ,  HAFNER MATHIAS DR

IPC: C07C237/22 ,  C07C317/44 ,  C07D295/215 ,  A61K31/195 ,  C07C315/04

公开(公告)号：CZ290684B6

公开(公告)日：2002-09-11

申请号：CZ287396

申请日：1995-03-23

Applicant: BASF AG

Inventor： BAUMANN ERNST DR ,  VOGELBACHER UWE JOSEF DR ,  RHEINHEIMER JOACHIM DR ,  KLINGE DAGMAR DR ,  RIECHERS HARTMUT DR ,  KROGER BURKHARD DR ,  BIALOJAN SIEGFRIED DR ,  BOLLSCHWEILER CLAUS DR ,  WERNER VOLFGANG DR ,  UNGER LILIANE DR ,  RASCHACK MANFRED DR

IPC: C07D251/26 ,  A61K31/00 ,  A61K31/505 ,  A61K31/506 ,  A61K31/53 ,  A61P9/00 ,  A61P9/08 ,  A61P9/10 ,  A61P9/12 ,  A61P11/08 ,  A61P13/02 ,  A61P15/00 ,  A61P25/04 ,  A61P39/02 ,  C07D239/26 ,  C07D239/34 ,  C07D239/38 ,  C07D401/12 ,  C07D405/12 ,  C07D409/12 ,  C07D413/12 ,  C07D417/12

Abstract: The present invention relates to the use of carboxylic acid derivatives of the general formula I for preparing medicament i.e. endothelin receptor antagonists. The medicament can be used for treating hypertension, renal insufficiency, and restenosis after angioplasty.

公开(公告)号：DE19738578A1

公开(公告)日：1999-03-11

申请号：DE19738578

申请日：1997-09-04

Applicant: BASF AG

Inventor： AMBERG WILHELM DR ,  JANSEN ROLF DR ,  KLINGE DAGMAR DR ,  RIECHERS HARTMUT DR ,  HERGENROEDER STEFAN DR ,  RASCHACK MANFRED DR ,  UNGER LILIANE DR

IPC: C07D239/34 ,  C07D239/52 ,  C07D277/34 ,  C07D409/12 ,  C07D491/052 ,  C07D239/24 ,  A61K31/215 ,  A61K31/41 ,  A61K31/495 ,  C07C59/64 ,  C07C69/734 ,  C07D233/32 ,  C07D239/80 ,  C07D239/96 ,  C07D263/22

Abstract: Carboxylic acid derivatives (I) and their salts and enantiomers are new. Carboxylic acid derivatives of formula (I) and their salts and enantiomers are new. R = tetrazole or COR1; R1 = OR7, 3-8C cycloalkyl, 1-8C alkyl, optionally substituted phenyl or benzyl, 3-6C alkenyl or optionally substituted 3-6C alkynyl; R7 = H, alkali or alkaline earth metal cation or organic ammonium ion; R2, R3 = H, OH, NH2, mono- or di(1-4C alkyl)amino, halo, 1-4C alkyl, 2-4C alkenyl, 2-4C alkynyl, 1-4C haloalkyl, 1-4C alkoxy, 1-4C haloalkoxy or 1-4C alkylthio; or CR2+CR10 = 5-6-membered ring; X, Y = N or CH; W = N or CR10; R10 = H or 1-4C alkyl; or CR10+CR2 or CR10+CR3 = 5-6-membered alkylene or alkenylene ring (optionally substituted and in which one or more of the methylene groups may be replaced by O, S, NH or N-(1-4C alkyl)); R4, R5 = optionally substituted phenyl or naphthyl (bound via a direct bond, methylene, ethylene, ethenylene, O, S, SO2, NH or N-alkyl) or optionally substituted 3-8C cycloalkyl; R6 = 3-8C cycloalkyl, phenyl, naphthyl or 5-6-membered heteroaromatic group containing 1-3 N atoms and/or an S or O atom (all optionally substituted); Z = O or S; B = 2-4C alkylene; Het = heterocyclic group of formula (i) or (ii); T = O, S or NR8; and R8 = 1-6C alkyl.

公开(公告)号：CZ104598A3

公开(公告)日：1998-09-16

申请号：CZ104598

申请日：1996-09-26

Applicant: BASF AG

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

IPC: A61K31/00 ,  A61K31/44 ,  A61K31/4427 ,  A61K31/443 ,  A61K31/444 ,  A61K31/505 ,  A61K31/53 ,  A61P5/24 ,  A61P5/36 ,  A61P5/42 ,  A61P9/12 ,  C07D213/74 ,  C07D239/10 ,  C07D239/42 ,  C07D239/46 ,  C07D239/48 ,  C07D239/50 ,  C07D239/52 ,  C07D239/58 ,  C07D251/46 ,  C07D401/04 ,  C07D405/12 ,  C07D405/14 ,  C07D471/04 ,  C07D487/04 ,  C07D491/052 ,  C07D491/056 ,  C07D239/70 ,  C07D487/02 ,  C07D251/42

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

公开(公告)号：CZ113297A3

公开(公告)日：1998-03-18

申请号：CZ113297

申请日：1995-10-07

Applicant: BASF AG

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

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 ,  A61K31/495

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：DE19536891A1

公开(公告)日：1997-04-10

申请号：DE19536891

申请日：1995-10-04

Applicant: BASF AG

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

IPC: A61K31/00 ,  A61K31/44 ,  A61K31/4427 ,  A61K31/443 ,  A61K31/444 ,  A61K31/505 ,  A61K31/53 ,  A61P5/24 ,  A61P5/36 ,  A61P5/42 ,  A61P9/12 ,  C07D213/74 ,  C07D239/10 ,  C07D239/42 ,  C07D239/46 ,  C07D239/48 ,  C07D239/50 ,  C07D239/52 ,  C07D239/58 ,  C07D251/46 ,  C07D401/04 ,  C07D405/12 ,  C07D405/14 ,  C07D471/04 ,  C07D487/04 ,  C07D491/052 ,  C07D491/056 ,  C07D251/12 ,  C07D405/06 ,  C07D403/06 ,  C07D491/044 ,  C07C229/02 ,  A61K31/495

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.