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公开(公告)号:DE19919218A1
公开(公告)日:2000-11-02
申请号:DE19919218
申请日:1999-04-28
Applicant: BASF AG
Inventor: KLING ANDREAS , LANGE UDO , LAUTERBACH ARNULF , GENESTE HERVE , SUBKOWSKI THOMAS , ZECHEL JOHANN-CHRISTIAN , DAX CLAUDIA ISABELLA
IPC: C07C275/42 , C07D263/34 , C07D277/48 , C07D277/56 , C07D307/68 , C07D333/38 , C07D409/12 , C07D413/12 , C07D417/12 , C07K5/078 , A61K38/05
Abstract: Peptide compounds (I) are new. Peptide derivatives of formula A-E-G-L (I) and their salts, prodrugs, enantiomers, diastereomers and tautomers are new. L = -N(R4)-CHR3-(CHR2)a-T; a = 0 or 1; T = COOH or group hydrolyzable to COOH; R2 = H, NHSO2R21, NHCOR21 or NHCOOR22; R21 = 1-6C alkyl, 3-6C cycloalkyl, (1-4C) alkyl-(3-6C) cycloalkyl, 5-12C bicycloalkyl or 6-18C tricycloalkyl (all optionally substituted (os)); or aryl, aralkyl, alkylheteroaryl or 3-6 membered (un)saturated or aromatic heterocycle (all os by 1-3 groups, two of which may together form a fused (un)saturated or aromatic heterocycle, itself os and optionally carrying a fused os (un)saturated or aromatic ring); R22 = alkyl, aryl, or alkylaryl (all os); R3 = H or -(CH2)b-(X)c-R31; b = 0-3; c = 0 or 1; X = SO2, S, O, CO, NHSO2, OCO, COO, NHCO, CONH, CON(R31), N(R31)CO, SO2NH, SO2N(R31) or N(R31)SO2; R31 = H or OH; 1-6C alkyl, alkoxy, arylalkoxy or aryloxy (all os); primary and optionally secondary or tertiary substituted amino; 2-6C alkenyl or 2-6C alkynyl (both os by 1-4C alkyl or aryl); 5-12C bicycloalkyl or 6-18C tricycloalkyl; or 3-6 membered (un)saturated heterocycle, 3-8C cycloalkyl, aryl or heteroaryl (all os by 1-3 groups, two of which may together form a fused (un)saturated or aromatic carbocycle or heterocycle, itself os and optionally carrying a fused os (un)saturated or aromatic ring); R4 = 1-4C alkyl, 3-6C alkenyl, 3-6C alkynyl or 3-6C cycloalkyl (all os); G = -N(R6)-CH((CH2)dR5)-CO-; d = 0-2;l R5 = as R31; or the side-chain of a natural aminoacid; R6 = H or as R4; E = -(NH)g-(CH2)t-Q-(CH2)e-CO-; e = 0-2; f, g = 0 or 1; Q = os heteroarylene (where two substituents may together form a fused (un)saturated or aromatic carbocycle or heterocycle, itself os and optionally carrying a fused os (un)saturated or aromatic ring); A = R10R11N-C(O)-, R10R11N-C(S)-, R10R11N-C(O)-, R12OC(O)- or R14N-C(=NR13)-; 2-pyridinyl, 2-pyrimidinyl or 4-pyrimidinyl, all substituted by R16 and R17; a diaza-heterocyclic group of formula (A1); a fused imidazole group of formula (A2); 3,4-dihydro-5H-1,3-thiazin-2-yl; uracil-6-yl; 1-aza-cyclopent-1-en-2-yl; 1-aza-cyclohex-1-en-2-yl; 1-aza-cyclohept-1-en-2-yl; or 5-oxo-4,5-dihydro-imidazol-2-yl; R10, R11 = H or -(CH2)h(X)i-R101; or NR10R11 = 3-8 membered os (un)saturated or aromatic heterocycle (optionally containing two further O, N or heteroatoms); h = 0-3; i = 0 or 1; R101 = as R31 but not H; R12 = alkyl, alkylaryl, 3-6C cycloalkyl, (1-4C) alkyl-(3-6C) cycloalkyl or aryl (all os); R13 = H, OH, CN or CONH2; or 1-4C alkyl, 1-4C alkoxy, -OCO-(1-4C) alkyl, alkylaryl, -O-alkylaryl, -OCO-aryl, -OCO-alkylaryl or -OCO-allyl (all os); R14 = H or (all os) 1-4C alkyl, -COO-(1-4C) alkyl, alkylaryl, -COO-alkylaryl, -COO-allyl, -CO-(1-4C) alkyl, -CO-alkylaryl or -CO-allyl; R15 = H or (all os) 1-4C alkyl, aryl or alkylaryl; R16, R17 = NH2, halo or (all os) 1-4C alkyl, 1-4C alkoxy or aryl; V = CH2CH2, CH=CH, 1,2-cyclohexylene, 1,2-cyclohex-1-enylene, (CH2)3 or CH2C(Me)2CH2; Z1-Z4 = CH, C(Me), C(Cl) or N; heterocycles contain 1-3 of O, S and/or N.
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公开(公告)号:TR9802042T2
公开(公告)日:2000-09-21
申请号:TR9802042
申请日:1997-04-04
Applicant: BASF AG
Inventor: AMBERG WILHELM , KLING ANDREAS , KLINGE DAGMAR , RIECHERS HARTMUT , BAUMANN ERNST , UNGER LILIANE , RASCHACK MANFRED , HERGENROEDER STEFAN , SCHULT SABINE
IPC: A61K31/00 , A61K31/47 , A61K31/505 , A61P9/00 , A61P9/12 , A61P13/00 , A61P13/12 , C07D215/22 , C07D215/227 , C07D239/34 , C07D239/60 , C07D401/12 , C07D403/12
CPC classification number: C07D215/227 , C07D239/34 , C07D239/60
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公开(公告)号:PL337507A1
公开(公告)日:2000-08-28
申请号:PL33750798
申请日:1998-06-05
Applicant: BASF AG
Inventor: AMBERG WILHELM , KLING ANDREAS , KLINGE DAGMAR , REICHERS HARTMUT , HERGENROEDER STEFAN , RASCHACK MANFRED , UNGER LILIANE
IPC: C07D251/16 , A61K31/4965 , A61K31/50 , A61K31/505 , A61K31/517 , A61K31/519 , A61K31/53 , A61P7/02 , A61P9/02 , A61P9/04 , A61P9/10 , A61P9/12 , A61P11/06 , A61P13/08 , A61P13/12 , A61P25/06 , A61P35/00 , A61P35/04 , A61P43/00 , C07C247/12 , C07D213/68 , C07D237/14 , C07D237/16 , C07D239/34 , C07D239/52 , C07D239/56 , C07D239/60 , C07D239/70 , C07D239/80 , C07D239/95 , C07D241/18 , C07D251/22 , C07D251/34 , C07D251/52 , C07D253/06 , C07D403/12 , C07D491/048 , C07C235/12
Abstract: The invention relates to carboxylic acid derivatives of formula (I) wherein the constituents have the meaning given in the description. The invention also relates to the production of said derivatives, and to their use as endothelin receptor antagonists.
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公开(公告)号:CO4930270A1
公开(公告)日:2000-06-27
申请号:CO97073662
申请日:1997-12-17
Applicant: BASF AG
Inventor: AMBERG WILHELM , JANSEN ROLF , KLING ANDREAS , KLINGE DAGMAR , RIECHERS HARTMUT , HERGENRODER STEFAN , RASCHACK MANFRED , UNGER LILIANE
IPC: C07D253/06 , A61K31/495 , A61K31/50 , A61K31/505 , A61K31/53 , A61P9/10 , A61P9/12 , A61P11/06 , A61P13/08 , C07D237/14 , C07D237/16 , C07D241/18 , C07D253/07 , C07D253/075 , C07D253/10 , C07D403/12 , C07D491/04
Abstract: Derivados de ácido carbónico de la fórmula I: CARACTERIZADOS porque R1 representa tetrazol o a un grupo en el que R tiene el siguiente significado: a) un residuo OR6 , en donde R6 significa: hidrógeno, el catión de un metal alcalino, el catión de metal alcalinotérreo, o un ión amonio fisiológicamente compatible; C3 -C8 cicloalquilo, C1 -C8 alquilo, CH2 -fenilo, que puede ser sustituido, un grupo C3 -C6 -alquenilo o C3 -C6 - alquinilo, que puede ser sustituido o fenilo, en caso dado, sustituido.b) un heteroaromático de 5 eslabones ligado con un átomo de nitrógeno, c) un grupo en el que k puede tomar los valores 0,1 y 2, p los valores 1, 2, 3 y 4 y R7 representa d) un residuo - 2 -donde R8 significa : C1 -C4 -alquilo, C3 -C8 -alquenilo, C3 -C8 -alquinilo, C3 -C8 -cicloalquilo, donde estos residuos pueden tener un residuo C1 -C4 -alcoxi, C1 -C4 -alquiltio y/o un residuo fenilo C1 -C4 -halogenalquilo o fenilo, en caso de ser necesario, sustituido; X nitrógeno o metino, con la condición de que si X = nitrógeno, entonces Z=nitrógeno y si X = metino, entonces por lo menos uno de los eslabones Y o Z son nitrógeno; Y nitrógeno o CR9 ; Z nitrógeno o CR10 , R2 C1 -C4 -alquilo, C2 -C4 -alquenilo, C2 -C4 -alquinilo, pudiendo estar estos residuos sustituidos; hidrógeno, halógeno, C1 -C4 -alcoxi, C1 -C4 -halogenalcoxi, C3 -C6 -alqueniloxi, C3 -C6 -alquiniloxi, C1 -C4 -alquiltio, C1 -C4 -alquilcarbonilo, C1 -C4 -coxicarbonilo, NH(C1 -C4 -alquilo) N(C1 -C4 -alquilo)2 , hidroxi, carboxi, ciano, amino; o CR2 junto con CR9 o CR10 forma un anillo de alquileno de 5 ó 6 eslabones o de alquenilo, que puede ser sustituido por uno o dos grupos C1 -C4 -alquilo y en donde uno o más grupos metilenos pueden ser sustituidos por oxígeno, azufre -NH o N(C1 -C4 -alquilo)2 . R3 y R4 (que pueden ser iguales o distintos) son: fenilo o naftilo, que pueden ser sustituidos fenilo o naftilo, que pueden estar unidos en posición orto por una unión directa a un grupo metileno, etileno o etenileno, a un átomo de oxígeno o azufre o a un grupo SO2 , NH- o N-alquilo; C3 -C8 -cicloalquilo, que puede ser sustituido; R5 hidrógeno, C1 -C8 alquilo, C3 -C8 -alquenilo o C3 -C8 -alquinilo, pudiendo estar estos residuos sustituidos; fenilo o naftilo, que pueden ser sustituidos; un heteroaromático de cinco a seis eslabones conteniendo de uno a tres átomos de nitrógeno y/o un átomo de azufre u oxígeno, el cual puede ser sustituido C3 -C8 -cicloalquilo, que puede ser sustituido R9 y R10 (que pueden ser iguales o diferentes) son:hidrógeno, hidroxi, NH2 , NH(C1 AND#8209;C4 AND#8209;alquilo), N(C1 AND#8209;C4 AND#8209;alquilo)2 , halógeno, C1 AND#8209;C4 alcoxi, C1 AND#8209;C4 AND#8209;halogenalcoxi o C1 AND#8209;C4 AND#8209;alquiltio; C1 AND#8209;C4 AND#8209;alquilo, C2 AND#8209;C4 AND#8209;alquenilo, C2 AND#8209;C4 AND#8209;alquinilo, pudiendo estos residuos estar sustituidos; o bien CR9 o CR10 está unido con CR2 como en R2 para dar un anillo de 5 o 6 eslabones;W es azufre, oxígeno o una unión simple; Q es oxígeno o nitrógeno, con la condición que en caso que Q = N, entonces W es una unión simple. así como las sales fisiológicamente compatibles y las formas enantiómeras y diastereómeras.
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公开(公告)号:NZ331704A
公开(公告)日:2000-06-23
申请号:NZ33170497
申请日:1997-04-04
Applicant: BASF AG
Inventor: AMBERG WILHELM , KLING ANDREAS , KLINGE DAGMAR , RIECHERS HARTMUT , BAUMANN ERNST , UNGER LILIANE , RASCHACK MANFRED , HERGENRODER STEFAN , SCHULT SABINE
IPC: A61K31/00 , A61K31/47 , A61K31/505 , A61P9/00 , A61P9/12 , A61P13/00 , A61P13/12 , C07D215/22 , C07D215/227 , C07D239/34 , C07D239/60 , C07D401/12 , C07D403/12
Abstract: These carboxylic acid derivatives, which are useful as inhibitors of endothelin receptors, are of the formula I where R is tetrazole, nitrile, COOH, R2 is H, OH, NH2, NHalkyl, N(alkyl)2, halo, alkyl, haloalkyl,alkoxy, haloalkoxy, alkylthio or CR2 is linked to CR12 to form a 5-6 membered ring; X is N or CR6, Y is N or CH, R3 is R2 or CR3 is linked to CR12 to form a 5-6 membered ring; R4 and R5 are generally optionally substituted phenyl or naphthyl; Z is S or O and R6 is selected from a wide group of substituents.
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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
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:TR200000132T2
公开(公告)日:2000-05-22
申请号:TR200000132
申请日:1998-07-07
Applicant: BASF AG
Inventor: JANSSEN BERND , BARLOZZARI TERESA , HAUPT ANDREAS , ZIERKE THOMAS , KLING ANDREAS
Abstract: Compounds of the present invention include cell growth inhibitors which are peptides of Formula I, A-B-D-E-F-(G)r-(K)s-L (I), and acid salts thereof, wherein A, B, D, E, F, G and K are α-amino acid residues, and s and r are each, independently, 0 or 1. L is a monovalent radical, such as, for example, an amino group, an N-substituted amino group, a &bgr;-hydroxylamino group, a hydrazido group, an alkoxy group, a thioalkoxy group, an aminoxy group, or an oximato group. The present invention also includes a method for treating cancer in a mammal, such as a human, comprising administering to the mammal an effective amount of a compound of Formula I in a pharmaceutically acceptable composition.
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公开(公告)号:PT758342E
公开(公告)日:2000-04-28
申请号:PT95917963
申请日:1995-04-26
Applicant: BASF AG
Inventor: JANSSEN BERND , ZIERKE THOMAS , ERNST BUSCHMANN DR , AMBERG WILHELM , BERNARD HARALD , HAUPT ANDREAS , JANITSCHKE LOTHAR , KARL ULRICH , KLING ANDREAS , MULLER STEFAN , POTZOLLI BERND DE , RITTER KURT , THYES MARCO
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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49.
公开(公告)号:CZ454399A3
公开(公告)日:2000-04-12
申请号:CZ454399
申请日:1998-06-05
Applicant: BASF AG
Inventor: AMBERG WILHELM , KLING ANDREAS , KLINGE DAGMAR , RIECHERS HARTMUT , HERGENROEDER STEFAN , RASCHACK MANFRED , UNGER LILIANE
IPC: A61K31/505 , A61P9/00 , A61P11/00 , A61P13/00 , A61P35/00 , C07C229/22 , C07C233/47 , C07C233/63 , C07C235/12 , C07C235/34 , C07C247/12 , C07D237/16 , C07D239/34 , C07D239/52 , C07D251/22 , C07D403/12
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公开(公告)号:CZ321399A3
公开(公告)日:2000-04-12
申请号:CZ321399
申请日:1998-03-05
Applicant: BASF AG
Inventor: RITTER KURT , AMBERG WILHELM , BARLOZZARI TERESA , HAUPT ANDREAS , JANNSEN BERN , KLING ANDREAS
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