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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.
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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.
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公开(公告)号：DE69425882T2
公开(公告)日：2001-01-11
申请号：DE69425882
申请日：1994-03-19
Applicant: BASF AG
Inventor： JANSSEN BERND , KLING ANDREAS , MUELLER STEFAN , RITTER KURT , SCHLECKER RAINER , KEILHAUER GERHARD , ROMERDAHL CYNTHIA , TRAUGOTT ULRICH
IPC: C07D295/08 , A61K31/34 , A61K31/341 , A61K31/357 , A61K31/36 , A61K31/40 , A61K31/403 , A61K31/41 , A61K31/42 , A61K31/421 , A61K31/4245 , A61K31/425 , A61K31/426 , A61K31/433 , A61K31/44 , A61K31/4402 , A61K31/4406 , A61K31/4409 , A61K31/4412 , A61K31/4418 , A61K31/445 , A61K31/451 , A61K31/47 , A61K31/495 , A61K31/496 , A61P35/00 , C07D207/32 , C07D207/333 , C07D209/52 , C07D211/14 , C07D213/30 , C07D215/14 , C07D261/08 , C07D261/18 , C07D263/14 , C07D263/32 , C07D271/06 , C07D271/10 , C07D277/24 , C07D285/12 , C07D295/092 , C07D307/42 , C07D307/58 , C07D317/58 , C07D317/66 , C07D333/06 , C07D333/16 , C07D413/12 , C07D417/12 , C07D521/00 , C07F9/6509
Abstract: This invention relates to 1-amino-3-phenoxy-propane-derivatives of formula 1: 1 (in which A, B, R, Rx, X and Z are defined as in the specification described) and methods for their preparation. These compounds may be used as modulators of multidrug resistance in cancer chemotherapy and for circumvention of resistance in the treatment of malaria.
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公开(公告)号：GR3031456T3
公开(公告)日：2000-01-31
申请号：GR990402545
申请日：1999-10-07
Applicant: BASF AG
Inventor： KARL ULRICH , MUELLER STEFAN , DE POTZOLLI BERND
IPC: C07B61/00 , C07C227/18 , C07C229/12 , C07C269/06 , C07C271/22 , C07C323/59
Abstract: A process for preparing N-protected N-alkylated amino acids of the formula I:in which the substituents have the meanings stated in the description, comprises mixing a compound of the formula IIwith a solution of potassium tert-butanolate in a non-protic organic solvent, and subsequently adding a C1-2-alkyl halide.
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公开(公告)号：ZA966371B
公开(公告)日：1998-01-26
申请号：ZA966371
申请日：1996-07-26
Applicant: BASF AG
Inventor： AMBERG WILHELM , BERNARD HARALD , BUSCHMANN ERNST , HAUPT ANDREAS , JANSSEN BERND , KARL ULRICH , KLING ANDREAS , MUELLER STEFAN , RITER KURT , ZIERKE THOMAS
IPC: C07K1/12 , C07K5/06 , C07K1/02 , C07K5/078 , C07K5/08 , C07K5/083 , C07K5/10 , C07K5/103 , C07K7/06 , A61K , C07K
Abstract: PCT No. PCT/EP96/03073 Sec. 371 Date Jan. 13, 1998 Sec. 102(e) Date Jan. 13, 1998 PCT Filed Jul. 12, 1996 PCT Pub. No. WO97/05162 PCT Pub. Date Feb. 13, 1997A process for preparing pentapeptides of the formula I where A and R1-R3 have the stated meanings, comprises assembling the pentapeptide stepwise starting from a prolinamide of the formula II where R1 and R2 have the abovementioned meanings, and eliminating the group -NR1R2 by hydrolysis where appropriate the peptide obtained in this way.
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Patent Agency Ranking
公开(公告)号：PL321159A1
公开(公告)日：1997-11-24
申请号：PL32115995
申请日：1995-04-26
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
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.
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公开(公告)号：SI9520061A
公开(公告)日：1997-06-30
申请号：SI9520061
申请日：1995-04-26
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
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.
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公开(公告)号：ZA9508642B
公开(公告)日：1997-04-14
申请号：ZA9508642
申请日：1995-10-13
Applicant: BASF AG
Inventor： RIECHERS HARTMUT , KLINGE DAGMAR , AMRBERG 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 , C07D , A61K
CPC classification number: C07D495/04 , C07D239/34 , C07D239/48 , C07D239/52 , C07D239/60 , C07D239/70 , C07D239/96 , C07D251/20 , C07D251/26 , C07D251/52 , C07D403/06 , C07D403/12 , C07D405/12 , C07D405/14 , C07D413/12 , C07D417/12 , C07D487/04 , C07D491/04 , C07D491/048
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公开(公告)号：HU9603068D0
公开(公告)日：1997-01-28
申请号：HU9603068
申请日：1995-04-26
Applicant: BASF AG
Inventor： AMBERG WILHELM , BERNARD HARALD , BUSCHMANN ERNST , DE POTZOLLI BERND , HAUPT ANDREAS , JANITSCHKE LOTHAR , JANSSEN BERND , KARL ULRICH , KLING ANDREAS , MUELLER STEFAN , RITTER KURT , THYES MARCO , ZIERKE THOMAS
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.
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公开(公告)号：DK0785926T3
公开(公告)日：2001-10-08
申请号：DK95935916
申请日：1995-10-07
Applicant: BASF AG
Inventor： KLING ANDREAS , MUELLER STEFAN , BAUMANN ERNST , RHEINHEIMER JOACHIM , UNGER LILIANE , KLINGE DAGMAR , RASCHACK MANFRED , WERNET WOLFGANG , RIECHERS HARTMUT , AMBERG WILHELM , 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.
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