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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.
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公开(公告)号：DE19745151A1
公开(公告)日：1999-04-15
申请号：DE19745151
申请日：1997-10-14
Applicant: BASF AG
Inventor： PUHL MICHAEL DR , AMBERG WILHELM DR , HILLEN HEINZ DR , KLING ANDREAS DR , HERGENROEDER STEFAN DR , MARKERT CLAUS OTTO DR
IPC: A61K38/00 , A61P1/00 , A61P9/00 , A61P9/04 , A61P9/10 , A61P9/12 , A61P11/06 , A61P13/08 , A61P13/12 , A61P25/06 , A61P35/00 , A61P43/00 , C07K1/06 , C07K5/065 , C07K5/078 , A61K38/05
Abstract: N-2-Mercapto-3-phenylpropionyl dipeptides of formula (I) and their salts are new. R1 = H or optionally substituted 1-8C alkyl, aryl(1-8C)alkyl, heteroaryl(1-8C)alkyl, aryl or heteroaryl; R2 = optionally substituted 2-thienylmethyl, 2-naphthylmethyl or N-Boc-3-indolylmethyl; and R3 = H or optionally substituted acyl.
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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.
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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.
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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.
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Patent Agency Ranking
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.
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公开(公告)号：DE4415998A1
公开(公告)日：1995-11-09
申请号：DE4415998
申请日：1994-05-06
Applicant: BASF AG
Inventor： AMBERG WILHELM DR , BERNARD HARALD DR , BUSCHMANN ERNST DR , HAUPT ANDREAS DR , JANITSCHKE LOTHAR DR , JANSSEN BERND DR , KARL ULRICH DR , KLING ANDREAS DR , MUELLER STEFAN DR , POTZOLLI BERND DE DR , RITTER KURT DR , ZIERKE THOMAS DR , THYES MARCO DR
Abstract: Compounds of formula (I) are disclosed, wherein R , R , R , and R have the meanings indicated in the description, as well as a process for the production of these compounds. The compounds are suitable for use as starting material for the synthesis of substances which have anti-tumour properties.
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公开(公告)号：DE4415997A1
公开(公告)日：1995-11-09
申请号：DE4415997
申请日：1994-05-06
Applicant: BASF AG
Inventor： AMBERG WILHELM DR , BERNARD HARALD DR , BUSCHMANN ERNST DR , HAUPT ANDREAS DR , JANITSCHKE LOTHAR DR , JANSSEN BERND DR , KARL ULRICH DR , KLING ANDREAS DR , MUELLER STEFAN DR , POTZOLLI BERND DE DR , RITTER KURT DR , ZIERKE THOMAS DR , THYES MARCO DR
Abstract: Disclosed is the compound Me2Val-Val-MeVal-Pro-Pro-NHBzl. HCl. The compound is produced from Z-Val-Val-MeVal-Pro-OR , wherein Z and R have the meanings indicated in the description. The compound disclosed has anti-neoplastic properties.
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公开(公告)号：CZ288448B6
公开(公告)日：2001-06-13
申请号：CZ326096
申请日：1995-04-26
Applicant: BASF AG
Inventor： AMBERG WILHELM DR , BERNARD HARALD DR , BUSCHMANN ERNST DR , HAUPT ANDREAS DR , JANITSCHKE LOTHAR DR , MUELLER STEFAN DR , DE POTZOLLI BERND DR , RITTER KURT DR , THYES MARCO DR , ZIERKE THOMAS DR , JANSSEN BERND DR , KARL ULRICH DR , KLING ANDREAS DR
Abstract: In the present invention, there is described pentapeptide hydrochloride of the formula Mei2Val-Val-MeVal-Pro-Pro-NHBz1.HCl, which is present in crystalline form. It is prepared from the compound of the formula Z-Val-Val-MeVal-Pro-ORe1, in which Z represents a benzyloxycarbonyl protecting group, which might be optionally substituted on the phenyl ring and Re1 represents alkyl containing 1 to 5 carbon atoms. In the present invention, there are also described intermediates for preparing the above indicated pentapeptide hydrochloride. The above-described compound exhibits antineoplastic activity.
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公开(公告)号：DE19750529A1
公开(公告)日：1999-05-20
申请号：DE19750529
申请日：1997-11-14
Applicant: BASF AG
Inventor： AMBERG WILHELM DR , JANSEN ROLF DR , HILLEN HEINZ DR , HERGENROEDER STEFAN DR , RASCHACK MANFRED DR , UNGER LILIANE DR
IPC: C07D249/12 , A61K31/41 , A61K31/415 , A61K31/4164 , A61K31/42 , A61K31/421 , A61K31/422 , A61K31/4245 , A61K31/425 , A61K31/426 , A61K31/427 , A61K31/428 , A61K31/433 , A61P9/04 , A61P9/08 , A61P9/10 , A61P9/12 , A61P11/06 , A61P13/08 , A61P13/12 , A61P35/00 , A61P43/00 , C07D231/20 , C07D233/70 , C07D261/12 , C07D263/38 , C07D271/06 , C07D271/10 , C07D273/01 , C07D275/02 , C07D275/03 , C07D277/20 , C07D277/32 , C07D277/34 , C07D277/60 , C07D277/68 , C07D285/00 , C07D285/08 , C07D285/12 , C07D291/04 , C07D413/12 , C07D417/12 , C07D263/20 , C07D277/72 , C07D263/46
Abstract: Heterocyclic alpha -hydroxycarboxylic acid derivatives (I) are new. Heterocyclic alpha -hydroxycarboxylic acid derivatives of formula (I) and their salts, enantiomers and diastereomers are new. R = tetrazolyl or CO-R; R = OR , a 5-membered heteroaromatic group bound via an N atom, -O-(CH2)p-S(O)k-R or -NH-SO2-R ; A = NR R , N3, OR , SR or 1-4C alkyl; X = O, S, CR or NR , provided that if X = CR , then Y = O, S or NR ; Y = O, S, CR or NR ; R , R = independently phenyl or naphthyl (which are optionally substituted or optionally bound via a methylene, ethylene, ethenylene, O, S, SO2, NH or N(1-4C alkyl) group) or 5- or 6C cycloalkyl; R , R = H, halo, or optionally substituted 1-4C alkoxy, 1-4C haloalkoxy, 3-6C alkenyloxy, 3-6C alkynyloxy, 1-4C alkylthio, (1-4C alkyl)carbonyl, (1-4C alkoxy)carbonyl, OH, NH2, NH(1-4C alkyl), N(1-4C alkyl)2, 1-4C alkyl, 2-4C alkenyl, 2-4C alkynyl, or CR and CR together form a 5- or 6-membered alkylene or alkenylene ring, which is optionally substituted and one or more of whose CH2 groups may be replaced by O, S, NH or N(1-4C alkyl); R = H, an alkali or alkaline earth metal cation or an organic ammonium ion, or 3-8C cycloalkyl, 1-8C alkyl, benzyl, 3-8C alkenyl, 3-8C alkynyl or optionally substituted phenyl; k = 0-2; p = 1-4; R = 1-4C alkyl, 3-8C cycloalkyl, 3-8C alkenyl, 3-8C alkynyl or optionally substituted phenyl; R = 1-4C alkyl, 3-8C cycloalkyl, 3-8C alkenyl, 3-8C alkynyl, 1-4C haloalkyl or phenyl (all optionally substituted); R = H, 1-8C alkyl, 3-8C alkenyl, 3-8C alkynyl or (1-5C alkyl)carbonyl, phenyl, naphthyl or 3-8C cycloalkyl (all optionally substituted), or R and R together form a 3-7C alkylene chain which may be substituted and whose alkylene chain may contain O or S atoms; R = H or 1-4C alkyl; R = H, 1-8C alkyl, 3-8C alkenyl, 3-8C alkynyl, phenyl, naphthyl or 3-8C cycloalkyl (all optionally substituted); R = H or 1-4C alkyl, or NR and CR together form a 5- or 6-membered alkylene or alkenylene ring, which is optionally substituted and one or more of whose CH2 groups may be replaced by O or S; R = H, halo, 1-4C alkyl, 2-4C alkenyl or 2-4C alkynyl (all optionally substituted); R = H or 1-4C alkyl.
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