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公开(公告)号：NO308846B1
公开(公告)日：2000-11-06
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
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：DK0691962T3
公开(公告)日：2000-10-16
申请号：DK94911931
申请日：1994-03-19
Applicant: BASF AG
Inventor： JANSSEN BERND , KLING ANDREAS , MUELLER STEFAN , RITTER KURT , KEILHAUER GERHARD , ROMERDAHL CYNTHIA , TRAUGOTT ULRICH , SCHLECKER RAINER
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：AT188485T
公开(公告)日：2000-01-15
申请号：AT95917963
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：DE59504450D1
公开(公告)日：1999-01-14
申请号：DE59504450
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: 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：HUT77443A
公开(公告)日：1998-04-28
申请号：HU9701975
申请日：1995-10-07
Applicant: BASF AG
Inventor： AMBERG WILHELM , BAUMANN ERNST , KLING ANDREAS , KLINGE DAGMAR , MUELLER STEFAN , RASCHACK MANFRED , RHEINHEIMER JOACHIM , RIECHERS HARTMUT , UNGER LILIANE , VOGELBACHER UWE JOSEF , WERNET WOLFGANG
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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Patent Agency Ranking
公开(公告)号：SI9520110A
公开(公告)日：1997-12-31
申请号：SI9520110
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.
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公开(公告)号：PL319655A1
公开(公告)日：1997-08-18
申请号：PL31965595
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.
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公开(公告)号：ZA958642B
公开(公告)日：1997-04-14
申请号：ZA958642
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
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：HU9603189D0
公开(公告)日：1997-01-28
申请号：HU9603189
申请日：1995-05-09
Applicant: BASF AG
Inventor： DE POTZOLLI BERND , KARL ULRICH , MUELLER STEFAN
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：ZA9503584B
公开(公告)日：1996-11-04
申请号：ZA9503584
申请日：1995-05-04
Applicant: BASF AG
Inventor： AMBERG WILHELM , BERNARD HARALD , BUSCHMANN ERNST , HAUPT ANDREAS , JANITSCHKE LOTHAR , JANSSEN BERND , KARL ULRICH , KLING ANDREAS , MUELLER STEFAN , POTZOLLI BERND DE , RITTER KURT , THYES MARCO , ZIERKE THOMAS
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