公开(公告)号：NO971675L

公开(公告)日：1997-06-10

申请号：NO971675

申请日：1997-04-11

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 ,  C07D291/04

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：CA2231500A1

公开(公告)日：1997-04-10

申请号：CA2231500

申请日：1996-09-26

Applicant: BASF AG

Inventor： KLINGE DAGMAR ,  KLING ANDREAS ,  UNGER LILIANE ,  RIECHERS HARTMUT ,  AMBERG WILHELM ,  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 ,  C07D473/00 ,  C07D491/04 ,  C07D401/12 ,  C07D403/12 ,  C07D401/14 ,  A61K31/195 ,  A61K31/215 ,  C07D251/26 ,  C07C229/36 ,  C07D239/47 ,  A61K31/535

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.

公开(公告)号：FI964446A

公开(公告)日：1997-01-03

申请号：FI964446

申请日：1996-11-05

Applicant: BASF AG

Inventor： AMBERG WILHELM ,  BERNARD HARALD ,  BUSCHMANN ERNST ,  HAUPT ANDREAS ,  JANITSCHKE LOTHAR ,  JANSSEN BERND ,  KARL ULRICH ,  KLING ANDREAS ,  MUELLER STEFAN ,  DE POTZOLLI BERND ,  RITTER KURT ,  THYES MARCO ,  ZIERKE THOMAS

IPC: A61K38/00 ,  A61P35/00 ,  C07K5/10 ,  C07K5/103 ,  C07K7/06 ,  C07K

Abstract: Compounds of the formulawhere R1, R2, R3 and R4 have the meaning stated in the description, and a process for preparing them are described. The compounds are suitable as starting material for synthesizing substances which are active against tumors.

公开(公告)号：FI964448A0

公开(公告)日：1996-11-05

申请号：FI964448

申请日：1996-11-05

Applicant: BASF AG

Inventor： AMBERG WILHELM ,  BERNARD HARALD ,  BUSCHMANN ERNST ,  HAUPT ANDREAS ,  JANITSCHKE LOTHAR ,  JANSSEN BERND ,  KARL ULRICH ,  KLING ANDREAS ,  MUELLER STEFAN ,  DE POTZOLLI BERND ,  RITTER KURT ,  THYES MARCO ,  ZIERKE THOMAS

IPC: A61K38/08 ,  A61K38/00 ,  A61P35/00 ,  C07K1/08 ,  C07K5/10 ,  C07K5/103 ,  C07K7/06 ,  C07K14/52 ,  C07K

Abstract: PCT No. PCT/EP95/01577 Sec. 371 Date Nov. 4, 1996 Sec. 102(e) Date Nov. 4, 1996 PCT Filed Apr. 26, 1995 PCT Pub. No. WO95/30691 PCT Pub. Date Nov. 16, 1995The compound Me2Val-Val-MeVal-Pro-Pro-NHBzlxHCl is described. It is prepared from Z-Val-Val-MeVal-Pro-OR1 where Z and R1 have the meanings stated in the description. The compound shows antineoplastic activity.

公开(公告)号：ZA953584B

公开(公告)日：1996-11-04

申请号：ZA953584

申请日：1995-05-04

Applicant: BASF AG

Inventor： BUSCHMANN ERNST ,  AMBERG WILHELM ,  BERNARD HARALD ,  HAUPT ANDREAS ,  JANSSEN BERND ,  KARL ULRICH ,  KLING ANDREAS ,  MUELLER STEFAN ,  JANITSCHKE LOTHAR ,  RITTER KURT ,  THYES MARCO ,  ZIERKE THOMAS ,  POTZOLLI BERND DE

IPC: A61K38/08 ,  A61P35/00 ,  A61K38/00 ,  C07K1/08 ,  C07K5/10 ,  C07K5/103 ,  C07K7/06 ,  C07K14/52 ,  C07K ,  A61K

Abstract: PCT No. PCT/EP95/01577 Sec. 371 Date Nov. 4, 1996 Sec. 102(e) Date Nov. 4, 1996 PCT Filed Apr. 26, 1995 PCT Pub. No. WO95/30691 PCT Pub. Date Nov. 16, 1995The compound Me2Val-Val-MeVal-Pro-Pro-NHBzlxHCl is described. It is prepared from Z-Val-Val-MeVal-Pro-OR1 where Z and R1 have the meanings stated in the description. The compound shows antineoplastic activity.

公开(公告)号：CA2201785A1

公开(公告)日：1996-04-25

申请号：CA2201785

申请日：1995-10-07

Applicant: BASF AG

Inventor： AMBERG WILHELM ,  KLING ANDREAS ,  RIECHERS HARTMUT ,  KLINGE DAGMAR ,  WERNET WOLFGANG ,  UNGER LILIANE ,  RASCHACK MANFRED ,  MUELLER STEFAN ,  BAUMANN ERNST ,  RHEINHEIMER JOACHIM ,  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: 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：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：HU0202646A2

公开(公告)日：2003-02-28

申请号：HU0202646

申请日：2000-07-05

Applicant: BASF AG

Inventor： AMBERG WILHELM ,  KETTSCHAU GEORG

IPC: A61K31/505 ,  A61K31/506 ,  A61K31/517 ,  A61P1/18 ,  A61P5/16 ,  A61P9/00 ,  A61P9/04 ,  A61P9/10 ,  A61P9/12 ,  A61P11/00 ,  A61P11/06 ,  A61P13/00 ,  A61P13/12 ,  A61P35/00 ,  A61P43/00 ,  C07D239/34 ,  C07D239/47 ,  C07D239/52 ,  C07D239/56 ,  C07D239/70 ,  C07D239/80 ,  C07D401/12 ,  C07D405/12 ,  C07D409/12 ,  C07D473/28

Abstract: The invention relates to compounds of formula (I), whereby the substituents have the meaning cited in the description. The invention also relates to the utilization of said derivatives.

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.