Dolastatin 15 derivatives
    323.
    发明专利

    公开(公告)号:AU4708199A

    公开(公告)日:2000-02-01

    申请号:AU4708199

    申请日:1999-06-23

    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.

    DOLASTATIN 15 DERIVATIVES
    324.
    发明专利

    公开(公告)号:CA2332641A1

    公开(公告)日:2000-01-20

    申请号:CA2332641

    申请日:1999-06-23

    Applicant: BASF AG

    Abstract: Compounds of the present invention include cell growth inhibitors which are peptides of Formula (I): A - B - D - E - F - G and acid salts thereof, where in A, D and E are .alpha.-amino acid residues, B is an .alpha.-amino acid resid ue 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 alkylen e 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 th e mammal an effective amount of a compound of Formula (I) in a pharmaceuticall y acceptable composition.

    New carboxylic acid derivatives
    328.
    发明专利

    公开(公告)号:DE19811915A1

    公开(公告)日:1999-09-23

    申请号:DE19811915

    申请日:1998-03-18

    Applicant: BASF AG

    Abstract: Carboxylic acid derivatives (I) and their salts and enantiomers are new. Carboxylic acid derivatives of formula R ZC(R )(BR )CH(R)OHet (I) and their salts and enantiomers are new. R = tetrazole or COR ; R = OR , 3-8C cycloalkyl, 1-8C alkyl, optionally substituted phenyl or benzyl, 3-6C alkenyl or optionally substituted 3-6C alkynyl; R = H, an alkali or alkaline earth metal cation or an organic ammonium ion; R = H, OH, NH2, NH-(1-4C alkyl), N-(1-4C alkyl)2, halo, 1-4C alkyl, 2-4C alkenyl, 2-4C alkynyl, 1-4C haloalkyl, 1-4C alkoxy, 1-4C haloalkoxy or 1-4C alkylthio, or CR and CR together form a 5- or 6-membered ring; X, Y = N or CH; W = N or CR ; R = H, halo or 1-4C alkyl, or CR and CR or CR together form a 5- or 6-membered alkylene or alkenylene ring which is optionally substituted and in which one or more of the methylene groups may be replaced by O, S, NH or N-(1-4C alkyl); R = as R ; R , R = optionally substituted phenyl or naphthyl (which may be bound via a direct bond, or via methylene, ethylene, ethenylene, O, S, SO2, NH or N-alkyl), or optionally substituted 3-8C cycloalkyl; R = H, 1-8C alkyl, 3-8C alkenyl or 3-8C alkynyl (optionally substituted by halo, OH, SH, COOH, NO2, NH2, CN, 1-4C alkoxy, 3-6C alkenyloxy, 3-6C alkynyloxy, 1-4C alkylthio, 1-4C haloalkoxy, (1-4C alkyl)carbonyl, (1-4C alkoxy)carbonyl, 3-8C alkylcarbonylalkyl, NH(1-4C alkyl), N(1-4C alkyl)2, 3-8C cycloalkyl, heteroaryloxy or heteroaryl ,where the aryl groups may themselves be substituted), 3-8C cycloalkyl (optionally substituted by halo, OH, SH, COOH, NO2, CN, 1-4C alkyl, 2-4C alkenyl, 2-4C alkynyl, 1-4C alkoxy, 1-4C alkylthio or 1-4C haloalkoxy), phenyl or naphthyl (both optionally substituted by halo, OH, NO2, NH2, CN, 1-4C alkyl, 1-4C haloalkyl, 1-4C alkoxy, 1-4C haloalkoxy, phenoxy, 1-4C alkylthio, NH(1-4C alkyl), N(1-4C alkyl)2, dioxymethylene or dioxoethylene), or a 5- or 6-membered heteroaromatic group containing 1-3 N atoms and/or a S or O atom (which is optionally substituted by 1-4 halo atoms and/or one or two 1-4C alkyl, 1-4C haloalkyl, 1-4C alkoxy, 1-4C haloalkoxy, 1-4C alkylthio, phenyl, phenoxy or benzoyl groups, where the phenyl rings may themselves be substituted); Z = O or S; B = 2-4C alkylene; Het = a heterocyclic group of formula (i) or (ii); T = O, S or NR ; R = 1-6C alkyl.

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