公开(公告)号：NO821018A

公开(公告)日：1982-09-28

申请号：NO821018

申请日：1982-03-26

Applicant: BASF AG

Inventor： BINNIG FRITZ ,  MUELLER CLAUS D ,  RASCHACK MANFRED ,  PHILIPSBORN GERDA VON

IPC: A61K31/435 ,  A61P9/00 ,  A61P9/06 ,  C07D471/08 ,  C07D

CPC classification number: C07D471/08

公开(公告)号：HRP20040364B1

公开(公告)日：2006-09-30

申请号：HRP20040364

申请日：2004-04-22

Applicant: BASF AG

Inventor： REICHERS HARTMUT ,  KLINGE DAGMAR ,  AMBERG WILHELM ,  KLING ANDREAS ,  MUELLER STEFAN ,  BAUMANN ERNST ,  RHEINHEIMER JOACHIM ,  VOGELBACHER UWE JOSEPH ,  WERNET WOLFGANG ,  UNGER LILIIANE ,  RASCHACK MANFRED

IPC: C07D239/60 ,  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 ,  C07D239/70 ,  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：HRP20040364A2

公开(公告)日：2005-06-30

申请号：HRP20040364

申请日：2004-04-22

Applicant: BASF AG

Inventor： REICHERS HARTMUT ,  KLINGE DAGMAR ,  AMBERG WILHELM ,  KLING ANDREAS ,  MUELLER STEFAN ,  BAUMANN ERNST ,  RHEINHEIMER JOACHIM ,  VOGELBACHER UWE JOSEPH ,  WERNET WOLFGANG ,  UNGER LILIIANE ,  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：NZ504316A

公开(公告)日：2002-12-20

申请号：NZ50431698

申请日：1998-10-16

Applicant: BASF AG

Inventor： AMBERG WILHELM ,  JANSEN ROLF ,  HERGENRODER 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 ,  C07D239/26 ,  C07D491/052 ,  C07D491/056 ,  C07D413/12

Abstract: A carboxylic acid derivative of formula (I) or a salt wherein: R1 is tetrazole or -C(O)-R; R is OR9, a 5-membered heteroaromatic ring system linked via a nitrogen atom; -O-(CH2)p-S(O)k-R10 or -NH-SO2-R11; R2 is H, OH, NH2, NH-alkyl, N(alkyl)2, halogen, alkyl, alkenyl, alkynyl, haloalkyl, alkoxy, haloalkoxy or alkylthio or CR2 is linked to CR12 to give a 5 or 6- membered ring; X is nitrogen or methine and Y is nitrogen or methine; Z is nitrogen or CR12 wherein two of X to Z are nitrogen and the other is methine of CR12; R3 is H, OH, NH2, NH-alkyl, N(alkyl)2, halogen, alkyl, alkenyl, alkynyl, haloalkyl, alkoxy, haloalkoxy or alkylthio or CR3 is linked to CR12 to give a 5 or 6- membered ring R4 and R5 are independently cycloalkyl; optionally substituted phenyl or naphthyl, which can be connected together in the ortho positions by a direct linkage, methylene, ethylene or ethenylene, oxygen, sulphur, SO2, NH or N-alkyl; R3 is -C(O)-NR13R14 or -C(R21)(R20)-N(R18)(R19); R7 and R8 are independently H or alkyl; W is O or S and the rest of the variables are as defined in the specification. The compound can be in enantiomerically pure or diastereomerically pure form and is useful for treating diseases where an endothelin level is elevated.

公开(公告)号：AU748610B2

公开(公告)日：2002-06-06

申请号：AU9533398

申请日：1998-08-24

Applicant: BASF AG

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

IPC: A61K31/421 ,  A61K31/426 ,  A61K31/428 ,  A61K31/496 ,  A61K31/505 ,  A61P9/10 ,  A61P9/12 ,  A61P43/00 ,  C07D239/34 ,  C07D239/52 ,  C07D263/38 ,  C07D277/20 ,  C07D277/34 ,  C07D277/68 ,  C07D409/12 ,  C07D239/04

Abstract: The invention relates to carboxylic acid derivatives of formula (I) wherein the radicals are defined in the description, and to the use of these derivatives as ETA/ETB endothelin-receptor antagonists.

公开(公告)号：HRP20010164A2

公开(公告)日：2002-04-30

申请号：HRP20010164

申请日：2001-03-08

Applicant: BASF AG

Inventor： AMBERG WILHELM ,  JANSEN ROLF ,  KETTSCHAU GEORG ,  HERGENROEDER STEFAN ,  RASCHACK MANFRED ,  UNGER LILIANE

IPC: C07D251/22 ,  A61K31/505 ,  A61K31/517 ,  A61K31/519 ,  A61K31/53 ,  A61K45/00 ,  A61P9/04 ,  A61P9/10 ,  A61P9/12 ,  A61P13/08 ,  A61P13/12 ,  A61P35/00 ,  A61P43/00 ,  C07D239/34 ,  C07D239/52 ,  C07D239/60 ,  C07D239/70 ,  C07D251/52 ,  C07D401/12 ,  C07D403/12 ,  C07D405/12 ,  C07D491/048 ,  C07D495/04

Abstract: The invention relates to new carboxylic acid derivatives of the formula (I), where the substituents have the meaning given in the description, their production and their use as endothelin-receptor antagonists.

公开(公告)号：PT752854E

公开(公告)日：2002-02-28

申请号：PT95914301

申请日：1995-03-23

Applicant: BASF AG

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

IPC: A61K31/00 ,  A61K31/505 ,  A61K31/506 ,  C07D251/26 ,  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: PCT No. PCT/EP95/01099 Sec. 371 Date Sep. 30, 1996 Sec. 102(e) Date Sep. 30, 1996 PCT Filed Mar. 23, 1995 PCT Pub. No. WO95/26716 PCT Pub. Date Oct. 12, 1995A method of inhibiting endothelin receptors by administering to a patient a compound of the formula I I

公开(公告)号：BG105618A

公开(公告)日：2002-01-31

申请号：BG10561801

申请日：2001-06-18

Applicant: BASF AG

Inventor： AMBERG WILHELM ,  JANSEN ROLF ,  KETTSCHAU GEORG ,  RIECHERS HARTMUT ,  BAUMANN ERNST ,  HERGENROEDER STEFAN ,  RASCHACK MANFRED ,  UNGER LILIANE

IPC: C07D251/24 ,  A61K31/505 ,  A61K31/506 ,  A61K31/53 ,  A61P9/04 ,  A61P9/10 ,  A61P9/12 ,  A61P13/08 ,  A61P13/12 ,  A61P15/10 ,  A61P35/00 ,  A61P43/00 ,  C07C229/34 ,  C07C233/87 ,  C07C235/52 ,  C07D239/34 ,  C07D251/22 ,  C07D401/12 ,  C07D491/048 ,  C07D239/60

Abstract: The invention relates to carboxylic acid derivatives of general formula wherein their substituents have the meanings given in the description, as well as to their preparation and application as endothelin-receptor antagonists. 10 claims

公开(公告)号：BG63389B1

公开(公告)日：2001-12-31

申请号：BG10236298

申请日：1998-04-01

Applicant: BASF AG

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

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 ,  C07D487/02 ,  C07D491/05 ,  C07D239/70 ,  C07D251/42

Abstract: The invention relates to derivatives of aminoacids with the formula where the radicals have the meanings listed in the description, as well as to their use as medicamentous forms. 4 claims

公开(公告)号：BG105236A

公开(公告)日：2001-12-31

申请号：BG10523601

申请日：2001-02-09

Applicant: BASF AG

Inventor： AMBERG WILHELM ,  JANSEN ROLF ,  KETTSCHAU GEORG ,  HERGENROEDER STEFAN ,  RASCHACK MANFRED ,  UNGER LILIANE

IPC: C07D251/22 ,  A61K31/505 ,  A61K31/517 ,  A61K31/519 ,  A61K31/53 ,  A61K45/00 ,  A61P9/04 ,  A61P9/10 ,  A61P9/12 ,  A61P13/08 ,  A61P13/12 ,  A61P35/00 ,  A61P43/00 ,  C07D239/34 ,  C07D239/52 ,  C07D239/60 ,  C07D239/70 ,  C07D251/52 ,  C07D401/12 ,  C07D403/12 ,  C07D405/12 ,  C07D491/048 ,  C07D495/04

Abstract: The invention relates to new carboxylic acid derivatives of formula where the substituents have the meaning given in the description, their production and their use as endothelin-receptor antagonists. 11 claims