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公开(公告)号:DE10039998A1
公开(公告)日:2002-02-21
申请号:DE10039998
申请日:2000-08-11
Applicant: BASF AG
Inventor: GENESTE HERVE , KLING ANDREAS , LAUTERBACH ARNULF , GRAEF CLAUDIA ISABELLA , SUBKOWSKI THOMAS , HORNBERGER WILFRIED
IPC: C07D401/12 , A61K31/55 , A61K45/00 , A61K45/06 , A61P3/10 , A61P3/14 , A61P5/18 , A61P7/02 , A61P7/10 , A61P9/00 , A61P9/10 , A61P9/12 , A61P9/14 , A61P13/12 , A61P17/02 , A61P17/06 , A61P19/00 , A61P19/02 , A61P19/10 , A61P29/00 , A61P31/04 , A61P31/10 , A61P31/12 , A61P33/00 , A61P35/00 , A61P35/04 , A61P41/00 , A61P43/00 , C07D277/28 , C07D403/12 , C07D471/04 , C07D211/26 , C07D227/04 , C07D247/00 , C07D495/04
Abstract: The invention relates to novel compounds which bind to integrin receptors, in particular as ligands for the alpha V beta 3 integrin receptor, the use thereof and pharmaceutical preparations containing said compounds.
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公开(公告)号:NZ502296A
公开(公告)日:2002-02-01
申请号:NZ50229698
申请日:1998-07-07
Applicant: BASF AG
Inventor: JANSSEN BERND , BARLOZZARI TERESA , HAUPT ANDREAS , ZIERKE THOMAS , KLING ANDREAS
Abstract: Compound of formula: A-B-D-E-F-(G)r-(K)s-L wherein: A is a proline derivative of formula IIa, wherein na is O to 3; Ra I hydrogen, or unsubstituted or fluorine-substituted normal, branched or cyclic C1-3-alkyl; R1a is hydrogen, C1-3 -alkyl, phenyl, or substituted phenyl; or Ra and R1a together form a propylene bridge; and R2a, R3a, R4a and R5a are each, independently, hydrogen or alkyl; or an alpha-amino acid derivative of Formula IIIa, Formula IVa, Formula Va, Formula VIa, Formula VIIa, Formula VIIIa, a 2-azabicyclo heptane-3-carboxylic acid derivative of Formula IXa, an amino acid derivative of Formula Xa; B is a valyl, isoleucyl, allo-isoleucyl, norvalyl, 2-tert-butylglycyl or 2-ethylglycyl residue; or an alpha-amino acid residue of Formula IIb; D is an N-alkylvalyl, N-alkyl-2-ethylglycyl, N-alkyl-2-tert-butylglycyl, N-alkylnorleucyl, N-alkylisoleucyl, N-alkyl-allo-isoleucyl or N-alkylnorvalyl residue; or an alpha-amino acid residue of Formula IId, Formula IIId; E is a prolyl, thiazolidinyl-4-carbonyl, homoprolyl, or hydroxyprolyl residue; or an alpha-amino acid residue of Formula IIe; or an aminocyclopentanecarboxylic acid residue of Formula IIIe, wherein Re is alkyl and R1e is hydrogen, or unsubstituted or fluorine-substituted alkyl; F is a prolyl, thiazolidinyl-4-carbonyl, homoprolyl or hydroxyprolyl residue; or an alpha-amino acid residue of Formula IIf; or a 2- or 3-aminocyclopentanecarboxylic acid residue of Formula IIIf; G is an alpha-amino acid residue of Formula IIg; K is an alpha-amino acid of Formula IIk; and L is a substituted or unsubstituted amino, hydrazido, aminoxy or oximato group; and r and s are independently, 0 or 1; provided that when s and r are 0 and A is of formula IIa where na is 0 or 1 and R1a, R2a, R3a, R4a and R5a are each hydrogen, L is a substituted or unsubstituted amino or hydrazido group .
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公开(公告)号:ZA200100169B
公开(公告)日:2002-01-08
申请号:ZA200100169
申请日:2001-01-08
Applicant: BASF AG
Inventor: RITTER KURT , JANSSEN BERND , HAUPT ANDREAS , KLING ANDREAS , TERESA BARLOZ-ZARI , AMBERG WILHELM
Abstract: Compounds of the present invention include cell growth inhibitors which are peptides of Formula IA-B-D-E-F-G(I)and acid salts thereof, wherein A, D, and E are alpha -amino acid residues, B is an alpha -amino acid residue or an alpha -hydroxy acid residue, F is an aminobenzoic acid residue or an aminocycloalkanecarboxylic acid residue, and G is a monovalent radical, such as, for example, a hydrogen atom, an amino group, an alkyl group, an alkylene alkyl ether, an alkylene alkyl thioether, an alkylene aldehyde, an alkylene amide, a beta -hydroxylamino group, a hydrazido group, an alkoxy group, a thioalkoxy group, an aminoxy group, an oximato group, an alkylene aryl group, an alkylene ester, an alkylene sulfoxide or an alkylene sulfone. Another aspect of the present invention includes pharmaceutical compositions comprising a compound of Formula I and a pharmaceutically acceptable carrier. An additional embodiment of the present invention is 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:NO20015237A
公开(公告)日:2001-12-21
申请号:NO20015237
申请日:2001-10-26
Applicant: BASF AG
Inventor: ZECHEL JOHANN-CHRISTIAN , KLING ANDREAS , GENESTE HERVE , LANGE UDO , LAUTERBACH ARNULF , GRAEF CLAUDIA ISABELLA , SUBKOWSKI THOMAS , HORNBERGER WILFRIED
IPC: C12N9/99 , A61K31/27 , A61K31/381 , A61K31/421 , A61K31/426 , A61K31/4406 , A61K31/443 , A61K31/4439 , A61K38/00 , A61K45/00 , A61K45/06 , A61P3/10 , A61P3/14 , A61P7/02 , A61P9/00 , A61P9/04 , A61P9/08 , A61P9/10 , A61P13/12 , A61P17/02 , A61P17/06 , A61P19/02 , A61P19/08 , A61P19/10 , A61P29/00 , A61P31/04 , A61P31/12 , A61P33/00 , A61P35/00 , A61P43/00 , C07C275/42 , C07D207/34 , C07D213/56 , C07D249/14 , C07D263/34 , C07D263/48 , C07D277/20 , C07D277/48 , C07D277/56 , C07D307/68 , C07D333/38 , C07D333/40 , C07D401/12 , C07D409/12 , C07D413/12 , C07D417/12 , C07K5/02 , C07K5/023 , A61K38/06
CPC classification number: C07D263/34 , A61K38/00 , A61K45/06 , C07D277/48 , C07D307/68 , C07D333/38 , C07D409/12 , C07D413/12 , C07D417/12 , C07K5/0202
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公开(公告)号:NO20015237D0
公开(公告)日:2001-10-26
申请号:NO20015237
申请日:2001-10-26
Applicant: BASF AG
Inventor: ZECHEL JOHANN-CHRISTIAN , KLING ANDREAS , GENESTE HERVE , LANGE UDO , LAUTERBACH ARNULF , GRAEF CLAUDIA ISABELLA , SUBKOWSKI THOMAS , HORNBERGER WILFRIED
IPC: C12N9/99 , A61K31/27 , A61K31/381 , A61K31/421 , A61K31/426 , A61K31/4406 , A61K31/443 , A61K31/4439 , A61K38/00 , A61K45/00 , A61K45/06 , A61P3/10 , A61P3/14 , A61P7/02 , A61P9/00 , A61P9/04 , A61P9/08 , A61P9/10 , A61P13/12 , A61P17/02 , A61P17/06 , A61P19/02 , A61P19/08 , A61P19/10 , A61P29/00 , A61P31/04 , A61P31/12 , A61P33/00 , A61P35/00 , A61P43/00 , C07C275/42 , C07D207/34 , C07D213/56 , C07D249/14 , C07D263/34 , C07D263/48 , C07D277/20 , C07D277/48 , C07D277/56 , C07D307/68 , C07D333/38 , C07D333/40 , C07D401/12 , C07D409/12 , C07D413/12 , C07D417/12 , C07K5/02 , C07K
Abstract: The invention relates to new compounds which bind to integrin receptors, as well as to their production, their use as integrin receptor antagonists and for the treatment of diseases, pharmaceutical preparations containing said compounds and pharmaceutical preparations containing at least one other active compound.
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公开(公告)号:NO20014876D0
公开(公告)日:2001-10-08
申请号:NO20014876
申请日:2001-10-08
Applicant: BASF AG
Inventor: HILLEN HEINZ , SCHMIDT MARTIN , MACK HELMUT , SEITZ WERNER , HAUPT ANDREAS , ZECHEL JOHANN-CHRISTIAN , KLING ANDREAS
IPC: A61K38/00 , C12N9/99 , A61K38/55 , A61P1/04 , A61P1/18 , A61P5/14 , A61P7/02 , A61P9/00 , A61P9/10 , A61P11/00 , A61P11/06 , A61P13/12 , A61P15/00 , A61P17/02 , A61P19/02 , A61P21/04 , A61P25/00 , A61P25/28 , A61P29/00 , A61P37/02 , C07B43/00 , C07D401/12 , C07D409/12 , C07K5/06 , C07K5/062 , C07K5/065 , C07K5/068 , C07K5/072 , C07K5/078 , C07K
Abstract: Peptide substances, their preparation and their use as complement inhibitors are described. These are in particular substances having a guanidine or amidine radical as a terminal group. In particular, inhibitors of the complement proteases C1s and C1r are described.
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公开(公告)号:DK0785926T3
公开(公告)日:2001-10-08
申请号:DK95935916
申请日:1995-10-07
Applicant: BASF AG
Inventor: KLING ANDREAS , MUELLER STEFAN , BAUMANN ERNST , RHEINHEIMER JOACHIM , UNGER LILIANE , KLINGE DAGMAR , RASCHACK MANFRED , WERNET WOLFGANG , RIECHERS HARTMUT , AMBERG WILHELM , VOGELBACHER UWE JOSEF
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:NO310651B1
公开(公告)日:2001-08-06
申请号:NO981002
申请日:1998-03-06
Applicant: BASF AG
Inventor: AMBERG WILHELM , KLING ANDREAS , KLINGE DAGMAR , RIECHERS HARTMUT , UNGER LILIANE , RASCHACK MANFRED , HERGENROEDER STEFAN , ELGER BERND , SCHULT SABINE
IPC: A61K31/00 , A61K31/19 , C07D317/02 , A61K31/192 , A61K31/34 , A61K31/341 , A61K31/343 , A61K31/35 , A61K31/352 , A61K31/357 , A61K31/36 , A61K31/435 , A61K31/44 , A61K31/505 , A61P9/00 , A61P9/08 , C07C53/134 , C07C57/30 , C07C57/32 , C07C57/38 , C07C59/64 , C07C69/616 , C07C69/734 , C07C255/00 , C07D213/55 , C07D213/64 , C07D221/04 , C07D239/26 , C07D239/34 , C07D239/52 , C07D239/70 , C07D257/04 , C07D307/79 , C07D317/50 , C07D317/60 , C07D319/02 , C07D319/18
Abstract: PCT No. PCT/EP96/03793 Sec. 371 Date Feb. 24, 1998 Sec. 102(e) Date Feb. 24, 1998 PCT Filed Aug. 29, 1996 PCT Pub. No. WO97/09294 PCT Pub. Date Mar. 13, 1997Carboxylic acid derivatives of the formula I here R1 is a tetrazole [sic], nitrile [sic], a group COOH or a radical which can be hydrolyzed to COOH, and the other substituents have the meaning explained in the description.
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公开(公告)号:AU736414B2
公开(公告)日:2001-07-26
申请号:AU4552497
申请日:1997-09-02
Applicant: BASF AG
Inventor: AMBERG WILHELM , JANSEN ROLF , KLING ANDREAS , KLINGE DAGMAR , RIECHERS HARTMUT , HERGENRODER STEFAN , RASCHACK MANFRED , UNGER LILIANE
IPC: A61K31/505 , A61K31/506 , A61K31/519 , A61P9/04 , A61P9/08 , A61P9/12 , A61P43/00 , C07C59/66 , C07C69/734 , C07D239/34 , C07D239/52 , C07D239/60 , C07D239/70 , C07D491/04 , C07D491/048
Abstract: The invention relates to carboxylic acid derivatives of the formula Iwhere the radicals have the meanings stated in the description, and to their use as drugs.
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公开(公告)号:CO5040228A1
公开(公告)日:2001-05-29
申请号:CO96047377
申请日:1996-09-05
Applicant: BASF AG
Inventor: AMBERG WILHELM , KLING ANDREAS , DAGMAR KLINGE , RIECHERS HARTMUT , UNGER UNGER , MANFRED RASCHACK , HERGENRODER STEFAN , BERND ELGER , SCHULT SABINE
IPC: C07D317/02 , A61K31/00 , A61K31/185 , A61K31/19 , A61K31/192 , A61K31/34 , A61K31/341 , A61K31/343 , A61K31/35 , A61K31/352 , A61K31/357 , A61K31/36 , A61K31/435 , A61K31/44 , A61K31/505 , A61P9/00 , A61P9/08 , C07C53/134 , C07C57/30 , C07C57/32 , C07C57/38 , C07C59/64 , C07C69/616 , C07C69/734 , C07C255/00 , C07D213/55 , C07D213/64 , C07D221/04 , C07D239/26 , C07D239/34 , C07D239/52 , C07D239/70 , C07D257/04 , C07D307/79 , C07D317/50 , C07D317/60 , C07D319/02 , C07D319/18
Abstract: Derivados del ácido carboxílico de la fórmula IEn la que R1 significa un tetrazol, nitrilo, un grupo COOH o un radical COOH hidrolizable, y los otros sustituyentes tienen los siguientes significados:R2 y R3 (que pueden ser idénticos o diferentes):Fenilo o naftilo, que puede estar sustituido por uno o varios de los siguientes radicales: Halógeno, ciano, NO2 , hidroxi, C1 -C4 -alquilo, C1 -C4 -halógenoalquilo, C1 -C4 -alcoxi, C1 -C4 - halógenoalcoxi, fenoxi, C1 -C4 -alquiltio, amino, benciloxi, C1 -C4 -dialquilamino; ó fenilo o naftilo que están unidos entre sí en posición orto por vía de un enlace directo, un grupo metileno, etileno o etinileno, un átomo de oxígeno o de azufre;R4 fenilo o naftilo, metilendioxifenilo, etilendioxifenilo, indanilo, indolilo, piridilo, benzopiranilo, furanilo, benzofuranilo, isooxazolilo, isotiazolilo, 1, 3, 4-tiadiazolilo, pirimidinilo, 2,3-dihidrobenzofuranilo, benzotienilo, quinolinilo, C3 -C7 -cicloalquilo, tienilo, oxazolilo, tiazolilo, que pueden estar sustituidos por uno o varios de los siguientes radicales: halógeno, ciano, hidroxi, NO2 , C1 -C4 alquilo, C1 -C4 -halógenoalquilo, C1 -C4 -alcoxi, C1 -C4 -halogenoalcoxi, fenoxi, C1 -C4 -alquiltio, amino, beciloxi, C1 -C4 - alquilamino o C1 -C4 -dialquilamino, pudiendo los radicales alquilo formar juntos un anillo;R5 C1 -C8 alquilo, C3 -C6 -alquenilo, C3 -C6 -alquinilo o C3 -C8 -cicloalquilo, cuyos radicales pueden estar mono o polisustituidos por: halógeno, C1 -C4 -alcoxi, C1 -C4 -alquiltio, C1 -C4 -alquilamino, di-C1 -C4 -alquilamino;fenilo, bencilo, 1-metilnaftilo, 2-metilnaftilo o naftilo, que puede estar sustituidos cada vez por uno o varios de los siguientes radicales: halógeno, ciano, hidroxi, amino, C1 -C4 -alquilo, C1 -C4 - alcoxi, fenoxi, C1 -C4 -alquiltio, dioximetileno o dioxoetileno;n 1 - 2.
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