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    TETRAPEPTIDE DERIVATIVES OF DOLASTATIN AS ANTITUMOR AGENTS
    1.
    发明申请
    TETRAPEPTIDE DERIVATIVES OF DOLASTATIN AS ANTITUMOR AGENTS 审中-公开
    DOLASTATIN作为抗肿瘤药物的四肽衍生物

    公开(公告)号：WO9804278A3

    公开(公告)日：2003-04-17

    申请号：PCT/EP9703898

    申请日：1997-07-21

    Applicant: BASF AG ,  BARLOZZARI TERESA ,  HAUPT ANDREAS ,  JANSSEN BERND ,  GRIESINGER CHRISTIAN ,  BELIK DANIEL ,  BORETZKY MICHAEL

    Inventor： BARLOZZARI TERESA ,  HAUPT ANDREAS ,  JANSSEN BERND ,  GRIESINGER CHRISTIAN ,  BELIK DANIEL ,  BORETZKY MICHAEL

    IPC: A61K38/00 ,  A61P35/00 ,  C07K4/00 ,  C07K5/02 ,  C07K5/027 ,  A61K38/04

    CPC classification number: C07K5/0205 ,  A61K38/00

    Abstract: The present invention provides antitumor peptides of formula (I): A-B-NR -CHD-CH(OCH3)-CH2CO-E-K and the acid salts thereof. A is an amino acid residue selected from the group consisting of N-methyl-D-prolyl, N-methyl-D-homoprolyl and N, N-dimethyl-2 -ethylphenylglycyl, or an amino acid residue of the formula R R N-CHX-CO, wherein R is a methyl group or an ethyl group, R is a hydrogen atom, a methyl group or an ethyl group, and X is an alkyl group. B is an amino acid residue selected from the group consisting of valyl, isoleucyl, leucyl, and 2-t-butylglycyl. R is a hydrogen atom or a methyl group. D is a normal or branched C2-C5-alkyl group. E is an amino acid residue selected from the group consisting of prolyl, homoprolyl, 5-methylprolyl, and phenylalanyl, or E is a residue derived from an amino acid comprising a pyrrolidine group. K is an alkoxy group or an amino group. An additional embodiment of the present invention is a method for treating a malignancy in a mammal, such as a human, comprising administering to the mammal an effective amount of a compound or compounds of the formula (I) in a pharmaceutically acceptable composition.

    Abstract translation: 本发明提供式（I）的抗肿瘤肽：A-B-NR 3 -CHD-CH（OCH 3）-CH 2 CO-E-K及其酸式盐。 A是选自N-甲基-D-脯氨酰基，N-甲基-D-正戊基和N，N-二甲基-2-乙基苯基甘氨酰或式R 1的氨基酸残基的氨基酸残基。 R 2为N-CHX-CO，其中R 1为甲基或乙基，R 2为氢原子，甲基或乙基，X为烷基。 B是选自缬氨酰基，异亮氨酰基，亮氨酰基和2-叔丁基甘氨酰基的氨基酸残基。 R 3是氢原子或甲基。 D是正链或支链C 2 -C 5 - 烷基。 E是选自脯氨酰基，同环戊基，5-甲基脯氨酰基和苯丙氨酰基的氨基酸残基，或E是衍生自包含吡咯烷基的氨基酸的残基。 K是烷氧基或氨基。 本发明的另一个实施方案是用于治疗哺乳动物（例如人）的恶性肿瘤的方法，其包括向所述哺乳动物施用有效量的药学上可接受的组合物中的式（I）化合物或化合物。

    TETRAPEPTIDE DERIVATIVES OF DOLASTATIN AS ANTITUMOR AGENTS
    4.
    发明公开
    TETRAPEPTIDE DERIVATIVES OF DOLASTATIN AS ANTITUMOR AGENTS 失效
    TETRA肽衍生物多拉司抗肿瘤剂

    公开(公告)号：EP0920325A2

    公开(公告)日：1999-06-09

    申请号：EP97918936

    申请日：1997-07-21

    Applicant: BASF AG

    Inventor： BARLOZZARI TERESA ,  HAUPT ANDREAS ,  JANSSEN BERND ,  GRIESINGER CHRISTIAN ,  BELIK DANIEL ,  BORETZKY MICHAEL

    IPC: A61K38/00 ,  A61P35/00 ,  C07K4/00 ,  C07K5/02 ,  A61K38/07

    CPC classification number: C07K5/0205 ,  A61K38/00

    Abstract: The present invention provides antitumor peptides of formula (I): A-B-NR3-CHD-CH(OCH¿3?)-CH2CO-E-K and the acid salts thereof. A is an amino acid residue selected from the group consisting of N-methyl-D-prolyl, N-methyl-D-homoprolyl and N, N-dimethyl-2 -ethylphenylglycyl, or an amino acid residue of the formula R?1R2¿N-CHX-CO, wherein R1 is a methyl group or an ethyl group, R2 is a hydrogen atom, a methyl group or an ethyl group, and X is an alkyl group. B is an amino acid residue selected from the group consisting of valyl, isoleucyl, leucyl, and 2-t-butylglycyl. R3 is a hydrogen atom or a methyl group. D is a normal or branched C¿2?-C5-alkyl group. E is an amino acid residue selected from the group consisting of prolyl, homoprolyl, 5-methylprolyl, and phenylalanyl, or E is a residue derived from an amino acid comprising a pyrrolidine group. K is an alkoxy group or an amino group. An additional embodiment of the present invention is a method for treating a malignancy in a mammal, such as a human, comprising administering to the mammal an effective amount of a compound or compounds of the formula (I) in a pharmaceutically acceptable composition.

    Dolastatin 15 derivatives
    8.
    发明专利
    Dolastatin 15 derivatives 未知

    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

    IPC: A61K38/00 ,  A61K38/08 ,  A61P35/00 ,  C07K7/06 ,  C12P19/34

    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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