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1. 发明申请

WO9722621A3 ANTINEOPLASTIC PEPTIDES 审中-公开
标题翻译：抗生素PEPTIDES
公开(公告)号：WO9722621A3
公开(公告)日：1998-02-26
申请号：PCT/EP9605518
申请日：1996-12-11
申请人： BASF AG , AMBERG WILHELM , BARLOZZARI TERESA , BERNARD HARALD , BUSCHMANN ERNST , HAUPT ANDREAS , HEGE HANS GUENTHER , JANSSEN BERND , KLING ANDREAS , LIETZ HELMUT , RITTER KURT , ULLRICH MARTINA , WEYMANN JUERGEN , ZIERKE THOMAS
发明人： AMBERG WILHELM , BARLOZZARI TERESA , BERNARD HARALD , BUSCHMANN ERNST , HAUPT ANDREAS , HEGE HANS-GUENTHER , JANSSEN BERND , KLING ANDREAS , LIETZ HELMUT , RITTER KURT , ULLRICH MARTINA , WEYMANN JUERGEN , ZIERKE THOMAS
IPC分类号： A61K38/00 , A61K31/00 , A61K38/08 , A61P35/00 , A61P35/02 , C07K1/00 , C07K7/06
CPC分类号： A61K38/08
摘要： Novel peptides of the following formula (I): R1R2N-CHX-CO-A-B-D-E-(G)¿s?-K in which R?1, R2¿, A, B, D, E, G, K, X, and s have the meanings stated in the description, and the preparation thereof are described. The novel peptides have an antineoplastic effect.

2. 发明申请

WO0118032A2 DOLASTATIN PEPTIDES 审中-公开
公开(公告)号：WO0118032A2
公开(公告)日：2001-03-15
申请号：PCT/US0024658
申请日：2000-09-08
申请人： BASF AG , UNIV ARIZONA , PETIT GEORGE R , SRIRANGAM JAYARAM K , WILLIAMS MICHAEL D , DURKIN KIERAN P M , BARLOZZARI TERESA , KLING ANDREAS , JANSSEN BERND , HAUPT ANDREAS
发明人： PETIT GEORGE R , SRIRANGAM JAYARAM K , WILLIAMS MICHAEL D , DURKIN KIERAN P M , BARLOZZARI TERESA , KLING ANDREAS , JANSSEN BERND , HAUPT ANDREAS
IPC分类号： C07K5/02 , C07K7/02 , C07K5/00
CPC分类号： C07K5/0202 , C07K5/0205 , C07K7/02
摘要： The present invention provides compounds of formula (I) where R1-R5 are each, independently, a hydrogen atom or a normal or branched C1-C6-alkyl group; A is a methionyl, phenylalanyl or phenylglycyl residue; n is 0 or 1; R6 is a hydrogen atom; and R7 is a carbocyclic group, an aromatic group, a C1-C4-alkyl group, a pyridylalkyl group or a heterocyclic group. In another embodiment, R6 is benzyl or -C(O)OR8, where R8 is a C1-C6-alkyl group, and R7 is a heteroaromatic group, such as a 2-thiazolyl group.
摘要翻译：本发明提供式（I）化合物，其中R 1 -R 5各自独立地为氢原子或正
或支链C 1 -C 6烷基; A是甲硫氨酰基，苯丙氨酰或苯基甘氨酰残基; n为0或1; R6是氢原子; 并且R 7是碳环基，芳基，C 1 -C 4 - 烷基，吡啶基烷基或杂环基。在另一个实施方案中，R 6为苄基或-C（O）OR 8，其中R 8为C 1 -C 6烷基，R 7为杂芳族基团，例如2-噻唑基。

3. 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。

4. 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.

5. 发明专利

CA2237721C ANTINEOPLASTIC PEPTIDES 未知
公开(公告)号：CA2237721C
公开(公告)日：2008-01-29
申请号：CA2237721
申请日：1996-12-11
申请人： BASF AG
发明人： RITTER KURT , ZIERKE THOMAS , BARLOZZARI TERESA , KLING ANDREAS , BUSCHMANN ERNST , BERNARD HARALD , HAUPT ANDREAS , HEGE HANS-GUENTHER , WEYMANN JURGEN , JANSSEN BERND , ULLRICH MARTINA , LIETZ HELMUT , AMBERG WILHELM
IPC分类号： A61K38/00 , C07K7/06 , A61K31/00 , A61K38/07 , A61K38/08 , A61P35/00 , A61P35/02 , C07K1/00 , C07K5/10
摘要： Novel peptides of the following formula (I): R1R2N-CHX-CO-A-B-D-E-(G)s-K in which R1, R2, A, B, D, E, G, K, X, and s have the meanings stated in the description, and the preparation thereof are described. The novel peptides have an antineoplastic effect.

6. 发明专利

BG64563B1 PEPTIDES, METHOD FOR THEIR PREPARATION AND APPLICATION 未知
公开(公告)号：BG64563B1
公开(公告)日：2005-07-29
申请号：BG10247998
申请日：1998-05-22
申请人： BASF AG
发明人： AMBERG WILHELM , BARLOZZARI TERESA , BERNARD HARALD , BUSCHMANN ERNST , HAUPT ANDREAS , HEGE HANS-GUENTHER , JANSSEN BERND , KLING ANDREAS , LIETZ HELMUT , RITTER KURT , ULLRICH MARTINA , WEYMANN JUERGEN , ZIERKE THOMAS
IPC分类号： A61K38/00 , A61K31/00 , A61K38/08 , A61P35/00 , A61P35/02 , C07K1/00 , C07K7/06
摘要： The invention relates to new peptides with the formula R1R2N-CHX-CO-A-B-D-E-(G)s-K, where R1, R2, A, B, D, E, G, K, X and s have the meanings listed in the description. The invention also relates to methods for the preparation of the above peptides having antineoplastic properties.

7. 发明专利

DE69815100D1 未知
公开(公告)号：DE69815100D1
公开(公告)日：2003-07-03
申请号：DE69815100
申请日：1998-03-09
申请人： BASF AG
发明人： BARLOZZARI TERESA , HAUPT ANDREAS
IPC分类号： A61K38/00 , A61K31/337 , A61K38/07 , A61K38/08 , A61K38/15 , A61P35/00 , C07K5/08 , C07K5/10 , C07K7/00 , A61K38/04
摘要： The present invention provides compositions and methods for the treatment of cancer in a subject wherein compounds of Formula I as defined herein in combination with paclitaxel, taxotere or modified taxane or taxoid analogs provide enhanced anticancer effects over the effects achieved with the individual compounds.

8. 发明专利

NZ502296A 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
申请人： BASF AG
发明人： JANSSEN BERND , BARLOZZARI TERESA , HAUPT ANDREAS , ZIERKE THOMAS , KLING ANDREAS
IPC分类号： A61K38/00 , A61K38/08 , A61P35/00 , C07K7/06 , C12P19/34
摘要： 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 .

9. 发明专利

HRP931504B1 NOVEL PEPTIDES, THEIR PRODUCTION AND USE 未知
公开(公告)号：HRP931504B1
公开(公告)日：2001-04-30
申请号：HRP931504
申请日：1993-12-16
申请人： BASF AG
发明人： HAUPT ANDREAS , JANSSEN BERND , RITTER KURT , KLINGE DAGMAR , KEILHAUER GERHARD , ROMERDAHL CYNTHIA , BARLOZZARI TERESA , QUIAN XIAO-DONG
IPC分类号： A61K38/00 , A61K38/08 , A61P35/00 , C07K1/00 , C07K5/02 , C07K5/027 , C07K7/02 , C07K7/06 , A61K38/07

10. 发明专利

AU731458B2 Antineoplastic peptides 未知
公开(公告)号：AU731458B2
公开(公告)日：2001-03-29
申请号：AU1192597
申请日：1996-12-11
申请人： BASF AG
发明人： AMBERG WILHELM , BARLOZZARI TERESA , BERNARD HARALD , BUSCHMANN ERNST , HAUPT ANDREAS , HEGE HANS-GUENTHER , JANSSEN BERND , KLING ANDREAS , LIETZ HELMUT , RITTER KURT , ULLRICH MARTINA , WEYMANN JURGEN , ZIERKE THOMAS
IPC分类号： A61K38/00 , A61K31/00 , A61K38/08 , A61P35/00 , A61P35/02 , C07K1/00 , C07K7/06
摘要： Novel peptides of the formula R R N-CHX-CO-A-B-D-E-(G)s-K in which R , R , A, B, D, E, G, K, X, and s have the meanings stated in the description, and the preparation thereof are described. The novel peptides have an antineoplastic effect.

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