公开(公告)号：HU220621B1

公开(公告)日：2002-03-28

申请号：HU9701975

申请日：1995-10-07

Applicant: BASF AG

Inventor： DR AMBERG WILHELM ,  DR BAUMANN ERNST ,  DR KLING ANDREAS ,  DR KLINGE DAGMAR ,  DR MUELLER STEFAN ,  DR RASCHACK MANFRED ,  DR RHEINHEIMER JOACHIM ,  DR RIECHERS HARTMUT ,  DR UNGER LILIANE ,  DR VOGELBACHER UWE JOSEF ,  DR 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.

公开(公告)号：HU221596B

公开(公告)日：2002-11-28

申请号：HU9603189

申请日：1995-05-09

Applicant: BASF AG

Inventor： DR DE POTZOLLI BERND ,  DR KARL ULRICH ,  DR 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.

公开(公告)号：HU220875B1

公开(公告)日：2002-06-29

申请号：HU9603067

申请日：1995-04-26

Applicant: BASF AG

Inventor： DR AMBERG WILHELM ,  DR BERNARD HARALD ,  DR BUSCHMANN ERNST ,  DR DE POTZOLLI BERND ,  DR HAUPT ANDREAS ,  DR JANITSCHKE LOTHAR ,  DR JANSSEN BERND ,  DR KARL ULRICH ,  DR KLING ANDREAS ,  DR MUELLER STEFAN ,  DR RITTER KURT ,  DR THYES MARCO ,  DR 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：HU220862B1

公开(公告)日：2002-06-29

申请号：HU9603068

申请日：1995-04-26

Applicant: BASF AG

Inventor： DR AMBERG WILHELM ,  DR BERNARD HARALD ,  DR BUSCHMANN ERNST ,  DR DE POTZOLLI BERND ,  DR HAUPT ANDREAS ,  DR JANITSCHKE LOTHAR ,  DR JANSSEN BERND ,  DR KARL ULRICH ,  DR KLING ANDREAS ,  DR MUELLER STEFAN ,  DR RITTER KURT ,  DR THYES MARCO ,  DR ZIERKE THOMAS

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

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.