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1. 发明申请

WO9804278A3 TETRAPEPTIDE DERIVATIVES OF DOLASTATIN AS ANTITUMOR AGENTS 审中-公开
标题翻译： 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
申请人： BASF AG , BARLOZZARI TERESA , HAUPT ANDREAS , JANSSEN BERND , GRIESINGER CHRISTIAN , BELIK DANIEL , BORETZKY MICHAEL
发明人： BARLOZZARI TERESA , HAUPT ANDREAS , JANSSEN BERND , GRIESINGER CHRISTIAN , BELIK DANIEL , BORETZKY MICHAEL
IPC分类号： A61K38/00 , A61P35/00 , C07K4/00 , C07K5/02 , C07K5/027 , A61K38/04
CPC分类号： C07K5/0205 , A61K38/00
摘要： 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.
摘要翻译：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。

2. 发明公开

EP0920325A2 TETRAPEPTIDE DERIVATIVES OF DOLASTATIN AS ANTITUMOR AGENTS 失效
标题翻译： 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
申请人： BASF AG
发明人： BARLOZZARI TERESA , HAUPT ANDREAS , JANSSEN BERND , GRIESINGER CHRISTIAN , BELIK DANIEL , BORETZKY MICHAEL
IPC分类号： A61K38/00 , A61P35/00 , C07K4/00 , C07K5/02 , A61K38/07
CPC分类号： C07K5/0205 , A61K38/00
摘要： 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.

3. 发明专利

ZA976725B Novel pentapeptides as antitumor agents 未知
公开(公告)号：ZA976725B
公开(公告)日：1999-02-12
申请号：ZA976725
申请日：1997-07-29
申请人： BASF AG
发明人： BARLOZZARI TERESA , HAUPT ANDREAS , GRIESINGER CHRISTIAN , JANSSEN BERND , BELIK DANIEL , BORETZKY MICHAEL , PETTIT GEORGE R
IPC分类号： A61K38/00 , A61P1/00 , A61P11/00 , A61P15/00 , A61P35/00 , C07K7/02 , C07K , A61K

4. 发明专利

ZA976723B Novel tetrapeptides as antitumor agents 未知
公开(公告)号：ZA976723B
公开(公告)日：1999-02-12
申请号：ZA976723
申请日：1997-07-29
申请人： BASF AG
发明人： BARLOZZARI TERESA , HAUPT ANDREAS , JANSSEN BERND , GRIESINGER CHRISTIAN , BELIK DANIEL , BORETZKY MICHAEL
IPC分类号： A61K38/00 , A61P35/00 , C07K4/00 , C07K5/02 , C07K , A61K
摘要： The present invention provides anti-tumor peptides of Formula I,A-B-NR3-CHD-CH(OCH3)-CH2CO-E-K(I),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 R1R2N-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 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 Formula I in a pharmaceutically acceptable composition.

5. 发明专利

ZA976724B Novel tetrapeptides as antitumor agents 未知
公开(公告)号：ZA976724B
公开(公告)日：1999-01-29
申请号：ZA976724
申请日：1997-07-29
申请人： BASF AG
发明人： BARLOZZARI TERESA , HAUPT ANDREAS , GRIESINGER BERND JANSSEN CHRIS , BELIK DANIEL , BORETZKY MICHAEL
IPC分类号： A61K38/00 , A61P35/00 , C07K4/00 , C07K5/02 , C07K , A61K
摘要： The present invention provides anti-tumor peptides of Formula I,A-B-NR3-CHD-CH(OCH3)-CH2CO-E-K(I),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 R1R2N-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 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 Formula I in a pharmaceutically acceptable composition.

6. 发明专利

ZA9706724B Novel tetrapeptides as antitumor agents 未知
公开(公告)号：ZA9706724B
公开(公告)日：1999-01-29
申请号：ZA9706724
申请日：1997-07-29
申请人： BASF AG
发明人： BARLOZZARI TERESA , HAUPT ANDREAS , GRIESINGER BERND JANSSEN CHRIS , BELIK DANIEL , BORETZKY MICHAEL
IPC分类号： A61K38/00 , A61P35/00 , C07K4/00 , C07K5/02 , C07K , A61K
CPC分类号： C07K5/0205 , A61K38/00

7. 发明专利

ZA9706725B Novel pentapeptides as antitumor agents 未知
公开(公告)号：ZA9706725B
公开(公告)日：1999-02-12
申请号：ZA9706725
申请日：1997-07-29
申请人： BASF AG
发明人： BARLOZZARI TERESA , HAUPT ANDREAS , GRIESINGER CHRISTIAN , JANSSEN BERND , BELIK DANIEL , BORETZKY MICHAEL , PETTIT GEORGE R
IPC分类号： A61K38/00 , A61P1/00 , A61P11/00 , A61P15/00 , A61P35/00 , C07K7/02 , C07K , A61K
CPC分类号： C07K7/02 , A61K38/00

8. 发明专利

ZA9706723B Novel tetrapeptides as antitumor agents 未知
公开(公告)号：ZA9706723B
公开(公告)日：1999-02-12
申请号：ZA9706723
申请日：1997-07-29
申请人： BASF AG
发明人： BARLOZZARI TERESA , HAUPT ANDREAS , JANSSEN BERND , GRIESINGER CHRISTIAN , BELIK DANIEL , BORETZKY MICHAEL
IPC分类号： A61K38/00 , A61P35/00 , C07K4/00 , C07K5/02 , C07K , A61K
CPC分类号： C07K5/0205 , A61K38/00

9. 发明专利

AU4296597A Tetrapeptide derivatives of dolastatin as antitumor agents 未知
公开(公告)号：AU4296597A
公开(公告)日：1998-02-20
申请号：AU4296597
申请日：1997-07-21
申请人： BASF AG
发明人： BARLOZZARI TERESA , HAUPT ANDREAS , JANSSEN BERND , GRIESINGER CHRISTIAN , BELIK DANIEL , BORETZKY MICHAEL
IPC分类号： A61K38/00 , A61P35/00 , C07K4/00 , C07K5/02 , A61K38/07
摘要： The present invention provides anti-tumor peptides of Formula I,A-B-NR3-CHD-CH(OCH3)-CH2CO-E-K(I),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 R1R2N-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 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 Formula I in a pharmaceutically acceptable composition.

10. 发明专利

AU3769297A Dolastatin pentapeptide derivatives and their use as antitumor agents 未知
公开(公告)号：AU3769297A
公开(公告)日：1998-02-20
申请号：AU3769297
申请日：1997-07-21
申请人： BASF AG
发明人： BARLOZZARI TERESA , HAUPT ANDREAS , JANSSEN BERND , GRIESINGER CHRISTIAN , BELIK DANIEL , BORETZKY MICHAEL , PETTIT GEORGE ROBERT
IPC分类号： A61K38/00 , A61P1/00 , A61P11/00 , A61P15/00 , A61P35/00 , C07K7/02 , A61K38/08

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