公开(公告)号：AU740351B2

公开(公告)日：2001-11-01

申请号：AU5659498

申请日：1997-12-04

Applicant: BASF AG

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

IPC: C07D253/06 ,  A61K31/495 ,  A61K31/50 ,  A61K31/505 ,  A61K31/53 ,  A61P9/10 ,  A61P9/12 ,  A61P11/06 ,  A61P13/08 ,  C07D237/14 ,  C07D237/16 ,  C07D241/18 ,  C07D253/07 ,  C07D253/075 ,  C07D253/10 ,  C07D403/12 ,  C07D491/04 ,  C07D253/08 ,  C07D241/20 ,  C07D237/18 ,  C07D237/20 ,  C07D237/22

Abstract: The present invention relates to carboxylic acid derivatives of the formula Iwhere the substituents have the meanings explained in the description, and to preparation and use as endothelin receptor antagonists.

公开(公告)号：DK0752854T3

公开(公告)日：2001-10-08

申请号：DK95914301

申请日：1995-03-23

Applicant: BASF AG

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

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：AT204568T

公开(公告)日：2001-09-15

申请号：AT95935916

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 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：BR9916331A

公开(公告)日：2001-09-11

申请号：BR9916331

申请日：1999-12-09

Applicant: BASF AG

Inventor： AMBERG WILHELM ,  JANSEN ROLF ,  KETTSCHAU GEORG ,  RIECHERS HARTMUT ,  BAUMANN ERNST ,  DER STEFAN HERGENR ,  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 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：HRP960400B1

公开(公告)日：2001-08-31

申请号：HRP960400

申请日：1996-09-03

Applicant: BASF AG

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

IPC: A61K31/00 ,  A61K31/19 ,  A61K31/192 ,  A61K31/34 ,  A61K31/341 ,  A61K31/343 ,  C07D317/02 ,  A61K31/35 ,  A61K31/352 ,  A61K31/357 ,  A61K31/36 ,  A61K31/435 ,  A61K31/44 ,  A61K31/505 ,  A61P9/00 ,  A61P9/08 ,  C07C53/134 ,  C07C57/30 ,  C07C57/32 ,  C07C57/38 ,  C07C59/64 ,  C07C69/616 ,  C07C69/734 ,  C07C255/00 ,  C07D213/55 ,  C07D213/64 ,  C07D221/04 ,  C07D239/26 ,  C07D239/34 ,  C07D239/52 ,  C07D239/70 ,  C07D257/04 ,  C07D307/79 ,  C07D317/50 ,  C07D317/60 ,  C07D319/02 ,  C07D319/18

Abstract: PCT No. PCT/EP96/03793 Sec. 371 Date Feb. 24, 1998 Sec. 102(e) Date Feb. 24, 1998 PCT Filed Aug. 29, 1996 PCT Pub. No. WO97/09294 PCT Pub. Date Mar. 13, 1997Carboxylic acid derivatives of the formula I here R1 is a tetrazole [sic], nitrile [sic], a group COOH or a radical which can be hydrolyzed to COOH, and the other substituents have the meaning explained in the description.

公开(公告)号：PL342806A1

公开(公告)日：2001-07-02

申请号：PL34280699

申请日：1999-02-25

Applicant: BASF AG

Inventor： AMBERG WILHELM ,  JANSEN ROLF ,  KLINGE DAGMAR ,  RIECHERS HARTMUT ,  HERGENROEDER 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 ,  C07D239/42 ,  C07D239/47 ,  C07D213/64 ,  A61K31/44

Abstract: The invention relates to carboxylic acid derivatives of formula (I), wherein R -R , Q, W, X, Y and Z have the meanings given in the description. The novel compounds are suitable for combating diseases.

公开(公告)号：BG63202B1

公开(公告)日：2001-06-29

申请号：BG10277098

申请日：1998-09-15

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: The invention relates to derivatives of caboxylic acids with the formula where the radicals have the meanings listed in the description well as to their preparation and to application as medicamentous forms. 10 claims

公开(公告)号：CZ20010437A3

公开(公告)日：2001-05-16

申请号：CZ20010437

申请日：1999-08-07

Applicant: BASF AG

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

IPC: A61K31/505 ,  A61P9/00 ,  C07D239/34 ,  C07D239/52 ,  C07D239/70 ,  C07D403/12

公开(公告)号：SK11512000A3

公开(公告)日：2001-04-09

申请号：SK11512000

申请日：1999-02-05

Applicant: BASF AG

Inventor： AMBERG WILHELM ,  JANSEN ROLF ,  KLING ANDREAS ,  KLINGE DAGMAR ,  RIECHERS HARTMUT ,  HERGENRODER 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：BG104577A

公开(公告)日：2001-03-30

申请号：BG10457700

申请日：2000-07-04

Applicant: BASF AG

Inventor： AMBERG WILHELM ,  JANSEN ROLF ,  KLING ANDREAS ,  KLINGE DAGMAR ,  RIECHERS HARTMUT ,  HERGENRODER 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 wherein the substituents have the following meaning: R1 = tetrazole or a group R = a radical OR7 a 5-member red heteroaromatic bonded by a nitrogen atom such as pyrrolyl, pyrazolyl, imidazolyl and trizolyl; R2, R3 = hydrogen, hydroxy, NH2, NH2(C1-C4-alkyl), N(C1-C4-alkyl)2, halogen,C1-C4-alkyl, C2-C4-alkenyl,C2-C4-alkinyl, C1-C4-hydoxyalkyl, C1-C4-alkpxy, C1-C4 halogen alkyl, C1-C4-alkoxy, C1-C4 halogen alkoxy, or C1-C4-alkylthio; X = halogen,C1-C4-halogen alkyl, hydroxy; R4 and R5 = phenyl or naphthyl, C3-C7-cycloalkyl, phenyl or naphthyl which are bonded in ortho position by a direct bond, a methylene, ethylene or ethylene group, an oxygen or sulfur atom or an SO2-NH or an N-alkyl group or a 5-membered or 6-membered heteroaromatic; R6 = hydrogen, phenyl or naphthyl, a five or six-membered heteroaromatic, C1-C8-alkyl,C3-C6-alkenyl,C3-C6 alkynyl or C3-C8-cycloalkyl, whereby said radicals can be substituted once or many times, with the proviso that R6 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. 8 claims