公开(公告)号：PT785926E

公开(公告)日：2002-02-28

申请号：PT95935916

申请日：1995-10-07

Applicant: BASF AG

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

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：NZ502660A

公开(公告)日：2002-02-01

申请号：NZ50266098

申请日：1998-08-24

Applicant: BASF AG

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

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 ,  A61K31/517 ,  A61K31/519 ,  C07D239/70 ,  C07D491/048

Abstract: A carboxylic acid derivative or a physiologically tolerated salts or enantiomerically pure forms thereof has the formula (I) wherein: R is tetrazole or -C(O)-R1; R1 is OR7, cycloalkyl, alkyl, or optionally substituted CH2-phenyl, alkenyl, alkynyl or phenyl; R4 and R5 are independently optionally substituted phenyl or naphthoyl or phenyl or naphthyl which are linked together in the ortho positions by a direct linkage, methylene, ethylene or ethenylene, oxygen, sulphur, SO2, NH or N-alkyl; R6 is H, or optionally substituted alkyl, alkenyl, alkynyl, phenyl, naphthyl, a five or six membered heteroaromatic system comprising one to three nitrogens and/or sulphur or oxygen or cycloalkyl; Z is sulphur or oxygen; B is alkylene; Het is a heterocyclic radical of formula Ia or Ib'; R2 is H, OH, N(R')2, halo, alkyl, alkenyl, alkynyl, haloalkyl, alkoxy, haloalkoxy, alkylthio or CR2 is linked to C10 to form a 5 or 6 membered ring defined below or if Het is a 5 membered ring, CR2 together with CR3 can be an optionally substituted 5- or 6- membered alkenyl or alkylenyl ring; X and Y are independently nitrogen or methane; W is nitrogen or CR10; R10 is H, halo or alkyl or CR10 forms together with CR2 or CR3 an optionally substituted 5 or 6 membered alkylene or alkenylene ring wherein one or more of the methylene groups can be replaced by oxygen, sulphur or NR'; R3 is H, OH, N(R')2, halo, alkyl, alkenyl, alkynyl, haloalkyl, alkoxy, halolkoxy, alkylthio or CR3 is linked to C10 to form a 5 or 6 membered ring defined above; R' is H or alkyl; T is O, S or NR8 and R8 is alkyl. A pharmaceutical composition thereof is useful as an endothelin receptor antagonist.

公开(公告)号：NO311802B1

公开(公告)日：2002-01-28

申请号：NO984713

申请日：1998-10-09

Applicant: BASF AG

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

IPC: A61K31/00 ,  A61K31/47 ,  A61K31/505 ,  A61P9/00 ,  A61P9/12 ,  A61P13/00 ,  A61P13/12 ,  C07D215/22 ,  C07D215/227 ,  C07D239/34 ,  C07D239/60 ,  C07D401/12 ,  C07D403/12

Abstract: PCT No. PCT/EP97/01687 Sec. 371 Date Oct. 8, 1998 Sec. 102(e) Date Oct. 8, 1998 PCT Filed Apr. 4, 1997 PCT Pub. No. WO97/38982 PCT Pub. Date Oct. 23, 1997Carboxylic acid derivatives of the formula I where the radicals have the meanings stated in the description, and the preparation of these agreements [sic] and their use as drugs are described.

公开(公告)号：SK832001A3

公开(公告)日：2001-11-06

申请号：SK832001

申请日：1999-08-07

Applicant: BASF AG

Inventor： AMBERG WILHELM ,  JANSEN ROLF ,  KETTSCHAU GEORG ,  HERGENRODER 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 ,  A61K31/503

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：DE59509541D1

公开(公告)日：2001-09-27

申请号：DE59509541

申请日：1995-10-07

Applicant: BASF AG

Inventor： RIECHERS HARTMUT ,  KLINGE DAGMAR ,  AMBERG WILHELM ,  KLING ANDREAS ,  MUELLER STEFAN ,  BAUMANN ERNST ,  RHEINHEIMER JOACHIM ,  VOGELBACHER 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：AT204471T

公开(公告)日：2001-09-15

申请号：AT95914301

申请日：1995-03-23

Applicant: BASF AG

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

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: 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：HRP20000602A2

公开(公告)日：2001-06-30

申请号：HRP20000602

申请日：2000-09-13

Applicant: BASF AG

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

IPC: A61K31/505 ,  A61K31/506 ,  A61P5/14 ,  A61P9/02 ,  A61P9/10 ,  A61P9/12 ,  A61P11/06 ,  A61P13/12 ,  A61P35/00 ,  A61P43/00 ,  C07D239/34 ,  C07D239/46 ,  C07D239/52 ,  C07D239/60 ,  C07D401/12 ,  C07D403/12 ,  C07D405/12 ,  C07D409/12 ,  C07D417/12 ,  C07D239/36

Abstract: The invention relates to carboxylic acid derivatives of formula (I), wherein the substituents have the following meanings; R = tetrazole or a group (1); R = a radical OR (2), (3), a 5-membe red heteroaromatic bonded by a nitrogen atom such a pyrrolyl, pyrazolyl, imidazolyl and trizolyl; R , R = hydrogen, hydroxy, NH2, NH(C1-C4-alkyl), N(C1-C4-alkyl)2, halogen, C1-C4-alkyl, C2-C4-alkenyl, C2-C4-alkinyl, C1-C4-hydroxyalkyl, C1-C4-alkoxy, C1-C4-halogen alkyl, C1-C4-alkoxy, C1-C4-halogen alkoxy or C1-C4-alkythio; X = halogen, C1-C4-halogen alkyl, hydroxy; R and R = phenyl or naphthyl, C3-C7-cycloalkyl, phenyl or naphthyl which are bonded in ortho position by a direct bond, a methylene, ethylene or ethenylene group, an oxygen or sulfur atom or an SO2-NH or an N-alkyl group or a 5-membered or 6-membered heteroaromatic; R = hydrogen, phenyl or naphthyl, a five or six-membered heteroaromatic, C1-C8-alkyl, C3-C6-alkenyl, C3-C6-alkinyl or C3-C8-cycloalkyl, whereby said radicals can be substituted once or many times, with the proviso that R can only stand for hydrogen if Z does not represent a single bond; Z = sulfur, oxygen or a single bond, in addition to the physiologically compatible salts and the enantiomeric-pure and diastereomeric-pure forms. The novel compounds are suitable for combating diseases, especially as endothelin antagonists.

公开(公告)号：NO20013000D0

公开(公告)日：2001-06-15

申请号：NO20013000

申请日：2001-06-15

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 ,  C07D

Abstract: The invention relates to carboxylic acid derivatives of formula (I), in which the substituents have the following meanings: R is tetrazol or a group (a); W and Z, can be identical or different and are nitrogen or methine, provided that if W and Z are methine, then Q is nitrogen; X is nitrogen or CR ; Y is nitrogen or CR ; Q is nitrogen or CR , provided that if Q is nitrogen then X is CR and Y is CR ; R and R are identical or different and are possibly substituted phenyl or naphthyl or phenyl or naphthyl which are linked in an ortho position via a direct bond, a methlyene, ethylene or ethenylene group, an oxygen or sulfur atom or a SO2-, NH- or N-alkyl group or possibly substituted C5-C6-cycloalkyl; R is a rest (b) or (c); and R is hydrogen, C1-C4-alkyl. The invention further relates to their preparation and their use as endothelin receptor antagonists. The invention also relates to compounds of formula (II) and a structural fragment of formula (d) in which the rests R , R , R , R and R have the meanings given in claim no. 1 and to their use as structural elements in an endothelin receptor antagonist.

公开(公告)号：PL342311A1

公开(公告)日：2001-06-04

申请号：PL34231199

申请日：1999-02-05

Applicant: BASF AG

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

IPC: A61K31/505 ,  A61K31/506 ,  A61P5/14 ,  A61P9/02 ,  A61P9/10 ,  A61P9/12 ,  A61P11/06 ,  A61P13/12 ,  A61P35/00 ,  A61P43/00 ,  C07D239/34 ,  C07D239/46 ,  C07D239/52 ,  C07D239/60 ,  C07D401/12 ,  C07D403/12 ,  C07D405/12 ,  C07D409/12 ,  C07D417/12 ,  A61P9/04

Abstract: The invention relates to carboxylic acid derivatives of formula (I), wherein the substituents have the following meanings; R = tetrazole or a group (1); R = a radical OR (2), (3), a 5-membe red heteroaromatic bonded by a nitrogen atom such a pyrrolyl, pyrazolyl, imidazolyl and trizolyl; R , R = hydrogen, hydroxy, NH2, NH(C1-C4-alkyl), N(C1-C4-alkyl)2, halogen, C1-C4-alkyl, C2-C4-alkenyl, C2-C4-alkinyl, C1-C4-hydroxyalkyl, C1-C4-alkoxy, C1-C4-halogen alkyl, C1-C4-alkoxy, C1-C4-halogen alkoxy or C1-C4-alkythio; X = halogen, C1-C4-halogen alkyl, hydroxy; R and R = phenyl or naphthyl, C3-C7-cycloalkyl, phenyl or naphthyl which are bonded in ortho position by a direct bond, a methylene, ethylene or ethenylene group, an oxygen or sulfur atom or an SO2-NH or an N-alkyl group or a 5-membered or 6-membered heteroaromatic; R = hydrogen, phenyl or naphthyl, a five or six-membered heteroaromatic, C1-C8-alkyl, C3-C6-alkenyl, C3-C6-alkinyl or C3-C8-cycloalkyl, whereby said radicals can be substituted once or many times, with the proviso that R can only stand for hydrogen if Z does not represent a single bond; Z = sulfur, oxygen or a single bond, in addition to the physiologically compatible salts and the enantiomeric-pure and diastereomeric-pure forms. The novel compounds are suitable for combating diseases, especially as endothelin antagonists.

公开(公告)号：BG104754A

公开(公告)日：2001-05-31

申请号：BG10475400

申请日：2000-09-07

Applicant: BASF AG

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

IPC: C07D251/22 ,  A61K31/192 ,  A61K31/216 ,  A61K31/505 ,  A61K31/506 ,  A61K31/519 ,  A61K31/53 ,  A61P9/04 ,  A61P9/06 ,  A61P9/10 ,  A61P9/12 ,  A61P11/06 ,  A61P13/08 ,  A61P13/12 ,  A61P35/00 ,  A61P43/00 ,  C07C59/66 ,  C07C59/68 ,  C07C69/734 ,  C07D213/63 ,  C07D239/34 ,  C07D239/52 ,  C07D239/60 ,  C07D405/12 ,  C07D491/048 ,  C07D403/12 ,  C07D213/64

Abstract: The compounds are suitable for the treatment of diseases related to the endothelial level. They are derivatives of the carbonic acid with the formula wherein R1-R6, Q, W, X, Y and Z have the meanings given in the description. The invention also relates to a method for their production. 9 claims