公开(公告)号：FI964607A

公开(公告)日：1997-01-16

申请号：FI964607

申请日：1996-11-18

Applicant: BASF AG

Inventor： KARL ULRICH ,  MUELLER STEFAN ,  DE POTZOLLI BERND

IPC: C07B61/00 ,  C07C227/18 ,  C07C229/12 ,  C07C269/06 ,  C07C271/22 ,  C07C323/59 ,  C07C

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.

公开(公告)号：FI964607A0

公开(公告)日：1996-11-18

申请号：FI964607

申请日：1996-11-18

Applicant: BASF AG

Inventor： KARL ULRICH ,  MUELLER STEFAN ,  DE POTZOLLI BERND

IPC: C07B61/00 ,  C07C227/18 ,  C07C229/12 ,  C07C269/06 ,  C07C271/22 ,  C07C323/59 ,  C07C

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.

公开(公告)号：CA2190656A1

公开(公告)日：1995-11-30

申请号：CA2190656

申请日：1995-05-09

Applicant: BASF AG

Inventor： KARL ULRICH ,  MUELLER STEFAN ,  DE POTZOLLI BERND

IPC: C07B61/00 ,  C07C227/18 ,  C07C229/12 ,  C07C269/06 ,  C07C271/22 ,  C07C323/59 ,  C07C229/02 ,  C07F7/10 ,  C07C319/20 ,  C07C323/60

Abstract: A process for producing N-protected N-alkylated amino acids of formula (I) is described in which the components have the meaning given in the description. In the process, to a compound of formula (II) is added a solution of potassiumtert.-butanolate in a non-proteinic organic solvent and then a C1-2-alkyl halide is added.

公开(公告)号：CA2189691A1

公开(公告)日：1995-11-16

申请号：CA2189691

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

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

Abstract: Compounds of formula (I) are disclosed, wherein R1, R2, R3, and R4 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.

公开(公告)号：CA2155759A1

公开(公告)日：1994-10-13

申请号：CA2155759

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 ,  C07D295/112 ,  C07D401/12 ,  C07D403/12 ,  C07D405/12 ,  C07D409/12 ,  A61K31/435 ,  C07D211/70

Abstract: This invention relates to 1-amino-3-phenoxy-propane-derivatives of formula (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 multi-drug resistance in cancer chemotherapy and for circumvention of resistance in the treatment of malaria.

公开(公告)号：HRP950517B1

公开(公告)日：2004-06-30

申请号：HRP950517

申请日：1995-10-13

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：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：GR3032630T3

公开(公告)日：2000-05-31

申请号：GR20000400328

申请日：2000-02-10

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

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：DE59507578D1

公开(公告)日：2000-02-10

申请号：DE59507578

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

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

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：DE59603295D1

公开(公告)日：1999-11-11

申请号：DE59603295

申请日：1996-07-12

Applicant: BASF AG

Inventor： AMBERG WILHELM ,  BERNARD HARALD ,  BUSCHMANN ERNST ,  HAUPT ANDREAS ,  JANSSEN BERND ,  ULRICH KARL ,  KLING ANDREAS ,  MUELLER STEFAN ,  RITTER KURT ,  ZIERKE THOMAS

IPC: C07K1/02 ,  C07K1/12 ,  C07K5/06 ,  C07K5/078 ,  C07K5/08 ,  C07K5/083 ,  C07K5/10 ,  C07K5/103 ,  C07K7/06

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.