公开(公告)号：FI964448A

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：FI964446A0

公开(公告)日：1996-11-05

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：DE19533023B4

公开(公告)日：2007-05-16

申请号：DE19533023

申请日：1995-09-07

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: C07D239/60 ,  C07D251/30 ,  A61K31/41 ,  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 ,  C07D409/12 ,  C07D413/12 ,  C07D417/12 ,  C07D487/04 ,  C07D491/04 ,  C07D491/044 ,  C07D491/048 ,  C07D495/04

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：SI9520061B

公开(公告)日：2002-02-28

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

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：GR3036931T3

公开(公告)日：2002-01-31

申请号：GR20010401798

申请日：2001-10-18

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：PL180652B1

公开(公告)日：2001-03-30

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

IPC: A61K38/08 ,  A61P35/00 ,  C07K1/08 ,  C07K5/10 ,  A61K38/00 ,  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：DE69425882D1

公开(公告)日：2000-10-19

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.

公开(公告)号：AT185349T

公开(公告)日：1999-10-15

申请号：AT96925744

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.

公开(公告)号：AT183994T

公开(公告)日：1999-09-15

申请号：AT95920008

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

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：HU9900089A2

公开(公告)日：1999-05-28

申请号：HU9900089

申请日：1996-10-30

Applicant: BASF AG

Inventor： AMBERG WILHELM ,  BARLOZZARI TERESA ,  BERNARD HARALD ,  BUSCHMANN ERNST ,  DE ARRUDA MONIKA ,  HAUPT ANDREAS ,  JANSSEN BERND ,  KLING ANDREAS ,  MUELLER STEFAN ,  RITTER KURT ,  ROBINSON SIMON ,  ZIERKE THOMAS

IPC: A61K38/00 ,  A61K31/00 ,  C07K7/06 ,  A61K38/08

Abstract: Novel peptides of the formulaA-B-D-E-F-L,wherein A, B, D, E, F, and L have the meanings stated in the specification, and their preparation are disclosed. The novel compounds are suitable for controlling diseases.