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1. 发明授权

US5807984A Oligopeptides, the preparation and use thereof 失效
标题翻译：寡肽，其制备和用途
公开(公告)号：US5807984A
公开(公告)日：1998-09-15
申请号：US554897
申请日：1995-11-09
申请人： Andreas Kling , Bernd Janssen , Wilhelm Amberg , Andreas Haupt , Kurt Ritter , Ernst Buschmann , Harald Bernard , Stefan Muller , Thomas Zierke , Teresa Barlozzari , Monika de Arruda , Simon Robinson
发明人： Andreas Kling , Bernd Janssen , Wilhelm Amberg , Andreas Haupt , Kurt Ritter , Ernst Buschmann , Harald Bernard , Stefan Muller , Thomas Zierke , Teresa Barlozzari , Monika de Arruda , Simon Robinson
IPC分类号： A61K38/00 , A61K31/00 , C07K7/06 , A61K38/03
CPC分类号： C07K7/06 , A61K38/00
摘要： Novel peptides of the formula A--B--D--E--F--L, wherein A, B, D, E, F, and L have the meanings stated in the specification, and their preparation are disclosed. The novel compounds are suitable for controlling diseases.
摘要翻译：式A-B-D-E-F-L的新肽，其中A，B，D，E，F和L具有说明书中所述的含义，并且公开了它们的制备。新型化合物适用于控制疾病。

2. 发明申请

US20060009392A1 Antineoplastic peptides 有权
标题翻译：抗肿瘤肽
公开(公告)号：US20060009392A1
公开(公告)日：2006-01-12
申请号：US11179074
申请日：2005-07-11
申请人： Wilhelm Amberg , Teresa Barlozzari , Harald Bernard , Ernst Buschmann , Andreas Haupt , Hans-Guenther Hege , Bernd Janssen , Andreas Kling , Helmut Lietz , Kurt Ritter , Martina Ullrich , Jurgen Weymann , Thomas Zierke
发明人： Wilhelm Amberg , Teresa Barlozzari , Harald Bernard , Ernst Buschmann , Andreas Haupt , Hans-Guenther Hege , Bernd Janssen , Andreas Kling , Helmut Lietz , Kurt Ritter , Martina Ullrich , Jurgen Weymann , Thomas Zierke
IPC分类号： A61K38/08
CPC分类号： C07K7/06 , A61K38/00 , C07K5/101 , C07K7/02
摘要： The present invention provides antineoplastic peptides of formula I, R1R2N—CHX—CO-A-B-D-E-(G)s-K I wherein R1, R2, X, A, B, D, E, G, K, and s have the meanings stated in the description. The compounds have antineoplastic activity.
摘要翻译：本发明提供了式I的抗肿瘤肽，<？in-line-formula description =“In-line formula”end =“lead”？> R＆lt; 2＆gt; N-CHX-CO-ABDE-（G）在线式描述=“在线公式”end =“tail”？>其中R 1， / SUP>，R 2，X，A，B，D，E，G，K和S具有说明书中所述的含义。该化合物具有抗肿瘤活性。

3. 发明授权

US08440626B2 Antineoplastic peptides 有权
标题翻译：抗肿瘤肽
公开(公告)号：US08440626B2
公开(公告)日：2013-05-14
申请号：US12869314
申请日：2010-08-26
申请人： Wilhelm Amberg , Teresa Barlozzari , Harald Bernard , Ernst Buschmann , Andreas Haupt , Hans-Guenther Hege , Bernd Janssen , Andreas Kling , Helmut Lietz , Kurt Ritter , Martina Ullrich , Jurgen Weymann , Thomas Zierke
发明人： Wilhelm Amberg , Teresa Barlozzari , Harald Bernard , Ernst Buschmann , Andreas Haupt , Hans-Guenther Hege , Bernd Janssen , Andreas Kling , Helmut Lietz , Kurt Ritter , Martina Ullrich , Jurgen Weymann , Thomas Zierke
IPC分类号： A61K38/00 , A61K38/08 , A61P35/00 , C07K7/00
CPC分类号： C07K7/06 , A61K38/00 , C07K5/101 , C07K7/02
摘要： The present invention provides antineoplastic peptides of formula I, I R1R2N-CHX-CO-A-B-D-E-(G)S-K wherein R1, R2, X, A, B, D, E, G, K and s have the meanings stated in the description. The compounds have antineoplastic activity.
摘要翻译：本发明提供式I的抗肿瘤肽I R1R2N-CHX-CO-ABDE-（G）SK，其中R1，R2，X，A，B，D，E，G，K和s具有说明书中所述的含义。该化合物具有抗肿瘤活性。

4. 发明授权

US07807779B2 Antineoplastic peptides 有权
标题翻译：抗肿瘤肽
公开(公告)号：US07807779B2
公开(公告)日：2010-10-05
申请号：US12079980
申请日：2008-03-31
申请人： Wilhelm Amberg , Teresa Barlozzari , Harald Bernard , Ernst Buschmann , Andreas Haupt , Hans-Guenther Hege , Bernd Janssen , Andreas Kling , Helmut Lietz , Kurt Ritter , Martina Ullrich , Jurgen Weymann , Thomas Zierke
发明人： Wilhelm Amberg , Teresa Barlozzari , Harald Bernard , Ernst Buschmann , Andreas Haupt , Hans-Guenther Hege , Bernd Janssen , Andreas Kling , Helmut Lietz , Kurt Ritter , Martina Ullrich , Jurgen Weymann , Thomas Zierke
IPC分类号： C07K7/00 , A61K38/00
CPC分类号： C07K7/06 , A61K38/00 , C07K5/101 , C07K7/02
摘要： The present invention provides antineoplastic peptides of formula I, R1R2N—CHX—CO—A—B-D-E-(G)s-K wherein R1, R2, X, A, B, D, E, G, K and s have the meanings stated in the description. The compounds have antineoplastic activity.
摘要翻译：本发明提供式I的抗肿瘤肽，R1R2N-CHX-CO-A-BDE-（G）sK，其中R1，R2，X，A，B，D，E，G，K和s具有描述。该化合物具有抗肿瘤活性。

5. 发明申请

US20080234205A1 Antineoplastic peptides 有权
标题翻译：抗肿瘤肽
公开(公告)号：US20080234205A1
公开(公告)日：2008-09-25
申请号：US12079980
申请日：2008-03-31
申请人： Wilhelm Amberg , Teresa Barlozzari , Harald Bernard , Ernst Buschmann , Andreas Haupt , Hans-Guenther Hege , Bernd Janssen , Andreas Kling , Helmut Lietz , Kurt Ritter , Martina Ullrich , Jurgen Weymann , Thomas Zierke
发明人： Wilhelm Amberg , Teresa Barlozzari , Harald Bernard , Ernst Buschmann , Andreas Haupt , Hans-Guenther Hege , Bernd Janssen , Andreas Kling , Helmut Lietz , Kurt Ritter , Martina Ullrich , Jurgen Weymann , Thomas Zierke
IPC分类号： A61K38/08 , A61P35/00
CPC分类号： C07K7/06 , A61K38/00 , C07K5/101 , C07K7/02
摘要： The present invention provides antineoplastic peptides of formula I, R1R2N—CHX—CO—A—B-D-E-(G)s-K wherein R1, R2, X, A, B, D, E, G, K and s have the meanings stated in the description. The compounds have antineoplastic activity.
摘要翻译：本发明提供了式I的抗肿瘤肽，<？in-line-formula description =“In-line formula”end =“lead”？> R＆lt; 2＆gt; N-CHX-CO-ABDE-（G） -K <？in-line-formula description =“In-line Formulas”end =“tail”？>其中R 1， / SUP>，R 2，X，A，B，D，E，G，K和s具有说明书中所述的含义。该化合物具有抗肿瘤活性。

6. 发明授权

US07368528B2 Antineoplastic peptides 有权
标题翻译：抗肿瘤肽
公开(公告)号：US07368528B2
公开(公告)日：2008-05-06
申请号：US11179074
申请日：2005-07-11
申请人： Wilhelm Amberg , Teresa Barlozzari , Harald Bernard , Ernst Buschmann , Andreas Haupt , Hans-Guenther Hege , Bernd Janssen , Andreas Kling , Helmut Lietz , Kurt Ritter , Martina Ullrich , Jurgen Weyman , Thomas Zierke
发明人： Wilhelm Amberg , Teresa Barlozzari , Harald Bernard , Ernst Buschmann , Andreas Haupt , Hans-Guenther Hege , Bernd Janssen , Andreas Kling , Helmut Lietz , Kurt Ritter , Martina Ullrich , Jurgen Weyman , Thomas Zierke
IPC分类号： C07K7/00 , A61K38/00
CPC分类号： C07K7/06 , A61K38/00 , C07K5/101 , C07K7/02
摘要： The present invention provides antineoplastic peptides of formula I, R1R2N—CHX—CO-A-B-D-E-(G)s-K I wherein R1, R2, X, A, B, D, E, G, K, and s have the meanings stated in the description. The compounds have antineoplastic activity.
摘要翻译：本发明提供了式I的抗肿瘤肽，<？in-line-formula description =“In-line formula”end =“lead”？> R＆lt; 2＆gt; N-CHX-CO-ABDE-（G）在线式描述=“在线公式”end =“tail”？>其中R 1， / SUP>，R 2，X，A，B，D，E，G，K和S具有说明书中所述的含义。该化合物具有抗肿瘤活性。

7. 发明授权

US5965537A Dolastatin 15 derivatives with carbonyl and heterocyclic functionalities at the C-terminus 失效
标题翻译：在C-末端具有羰基和杂环官能团的Dolastatin 15衍生物
公开(公告)号：US5965537A
公开(公告)日：1999-10-12
申请号：US814577
申请日：1997-03-10
申请人： Kurt Ritter , Wilhelm Amberg , Teresa Barlozzari , Andreas Haupt , Bernd Janssen , Andreas Kling
发明人： Kurt Ritter , Wilhelm Amberg , Teresa Barlozzari , Andreas Haupt , Bernd Janssen , Andreas Kling
IPC分类号： A61K38/00 , A61P35/00 , A61P35/02 , C07K5/10 , C07K5/103 , C07K7/02 , C07K5/00
CPC分类号： C07K5/101 , C07K5/1027 , C07K7/02 , A61K38/00
摘要： The present invention relates to novel peptides useful as anti-cancer agents. The compounds of the invention are of Formula I,A-B-D-E-F-G (I)A, B, D, and E are .alpha.-amino acid residues. In one embodiment, F is an azacycloalkanecarboxylic acid residue. In this embodiment, G is a monovalent radical, for example, a hydrogen atom, an alkyl group, an aryl group, or a heteroaryl group. In another embodiment, F is an azacycloalkyl group and G is a heteroaryl group connected to F by a carbon-carbon bond.In another embodiment, the invention includes 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.
摘要翻译：本发明涉及可用作抗癌剂的新型肽。本发明的化合物是式I，A-B-D-E-F-G（I）A，B，D和E是α-氨基酸残基。在一个实施方案中，F是氮杂环烷羧酸残基。在本实施方案中，G是一价基团，例如氢原子，烷基，芳基或杂芳基。在另一个实施方案中，F是氮杂环烷基，G是通过碳 - 碳键与F连接的杂芳基。在另一个实施方案中，本发明包括用于治疗哺乳动物（例如人）中的癌症的方法，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。

8. 发明授权

US5985837A Dolastatin 15 derivatives 失效
标题翻译： Dolastatin 15衍生物
公开(公告)号：US5985837A
公开(公告)日：1999-11-16
申请号：US112249
申请日：1998-07-08
申请人： Kurt Ritter , Bernd Janssen , Andreas Haupt , Andreas Kling , Teresa Barlozzari , Wilhelm Amberg
发明人： Kurt Ritter , Bernd Janssen , Andreas Haupt , Andreas Kling , Teresa Barlozzari , Wilhelm Amberg
IPC分类号： A61K38/00 , A61K35/56 , A61P35/00 , C07K5/103 , C07K5/117 , C07K7/02 , A61K38/04 , A61K38/07 , A61K38/08 , C07K7/04
CPC分类号： C07K7/02 , C07K5/101 , C07K5/1024 , A61K38/00
摘要： 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.
摘要翻译：本发明的化合物包括作为式IA-BDEFG（I）的肽及其酸式盐的细胞生长抑制剂，其中A，D和E是α-氨基酸残基，B是α-氨基酸残基或α - 羟酸残基，F是氨基苯甲酸残基或氨基环烷烃羧酸残基，G是一价基团，例如氢原子，氨基，烷基，亚烷基烷基醚，亚烷基烷基硫醚，亚烷基醛，亚烷基酰胺，β-羟基氨基，酰肼基，烷氧基，硫代烷氧基，氨氧基，肟基，亚烷基芳基，亚烷基酯，亚烷基亚砜或亚砜。本发明的另一方面包括包含式I化合物和药学上可接受的载体的药物组合物。本发明的另一个实施方案是用于治疗哺乳动物（例如人）中的癌症的方法，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。

9. 发明授权

US07662786B2 Dolastatin 15 derivatives 有权
标题翻译： Dolastatin 15衍生物
公开(公告)号：US07662786B2
公开(公告)日：2010-02-16
申请号：US11406512
申请日：2006-04-18
申请人： Bernd Janssen , Teresa Barlozzari , Andreas Haupt , Thomas Zierke , Andreas Kling
发明人： Bernd Janssen , Teresa Barlozzari , Andreas Haupt , Thomas Zierke , Andreas Kling
IPC分类号： A61K38/00
CPC分类号： C07K7/06 , A61K38/00 , C12P19/34
摘要： Compounds of the present invention include cell growth inhibitors which are peptides of Formula I, A-B-D-E-F-(G)r-(K)s-L (I), and acid salts thereof, wherein A, B, D, E, F, G and K are α-amino acid residues, and s and r are each, independently, 0 or 1. L is a monovalent radical, such as, for example, an amino group, an N-substituted amino group, a β-hydroxylamino group, a hydrazido group, an alkoxy group, a thioalkoxy group, an aminoxy group, or an oximato group. The present invention also includes 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.
摘要翻译：本发明的化合物包括作为式I的肽，ABDEF-（G）r-（K）sL（I）及其酸式盐的细胞生长抑制剂，其中A，B，D，E，F，G和K 是α-氨基酸残基，s和r各自独立地为0或1.L为单价基团，例如氨基，N-取代氨基，β-羟基氨基，酰肼基，烷氧基，硫代烷氧基，氨氧基或肟基。本发明还包括用于治疗哺乳动物（例如人）中的癌症的方法，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。

10. 发明授权

US06458765B1 Dolastatin 15 derivatives 有权
标题翻译： Dolastatin 15衍生物
公开(公告)号：US06458765B1
公开(公告)日：2002-10-01
申请号：US09618694
申请日：2000-07-18
申请人： Bernd Janssen , Teresa Barlozzari , Andreas Haupt , Thomas Zierke , Andreas Kling
发明人： Bernd Janssen , Teresa Barlozzari , Andreas Haupt , Thomas Zierke , Andreas Kling
IPC分类号： A61K3800
CPC分类号： C07K7/06 , A61K38/00 , C12P19/34
摘要： Compounds of the present invention include cell growth inhibitors which are peptides of Formula I, A-B-D-E-F-(G)r-(K)s-L (I), and acid salts thereof, wherein A, B, D, E, F, G and K are &agr;-amino acid residues, and s and r are each, independently, 0 or 1. L is a monovalent radical, such as, for example, an amino group, an N-substituted amino group, a &bgr;-hydroxylamino group, a hydrazido group, an alkoxy group, a thioalkoxy group, an aminoxy group, or an oximato group. The present invention also includes 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.
摘要翻译：本发明的化合物包括作为式I的肽的细胞生长抑制剂及其酸式盐，其中A，B，D，E，F，G和K是α-氨基酸残基，s和r各自独立地，0或1. L是一价基团，例如氨基，N-取代氨基，β-羟基氨基，酰肼基，烷氧基，硫代烷氧基，氨氧基，或喔ato组。本发明还包括用于治疗哺乳动物（例如人）中的癌症的方法，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。

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