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1. 发明授权

US08163698B2 Dolastatin 15 derivatives 有权
标题翻译： Dolastatin 15衍生物
公开(公告)号：US08163698B2
公开(公告)日：2012-04-24
申请号：US12648446
申请日：2009-12-29
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 , A61K38/08
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，对 - 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。

2. 发明申请

US20120095012A1 TOLUIDINE SULFONAMIDES AND THEIR USE 审中-公开
标题翻译：托洛芬磺酰胺及其用途
公开(公告)号：US20120095012A1
公开(公告)日：2012-04-19
申请号：US13142518
申请日：2009-12-30
申请人： Jorge Alonson , Arantxa Encinas Lopez , Marcel Muelbaier , Jochen Ammenn , Bernd Wendt , Joe Lewis , Christoph Schultes , Bernd Janssen
发明人： Jorge Alonson , Arantxa Encinas Lopez , Marcel Muelbaier , Jochen Ammenn , Bernd Wendt , Joe Lewis , Christoph Schultes , Bernd Janssen
IPC分类号： A61K31/4436 , A61K31/381 , C07D213/71 , A61K31/44 , C07D333/34 , A61K31/4178 , C07D413/12 , A61K31/422 , A61P9/10 , A61P19/02 , A61P11/06 , A61P1/00 , A61P17/06 , A61P37/06 , A61P35/00 , A61P7/00 , A61P35/02 , A61K31/443 , A61K31/506 , C07D401/12 , A61K31/4439 , A61K31/501 , C07D403/12 , A61K31/4025 , A61K31/4245 , A61K31/444 , A61P17/00 , A61P29/00 , C07D409/12
CPC分类号： C07D409/12 , C07D207/36 , C07D213/71 , C07D239/38 , C07D241/18 , C07D307/64 , C07D333/34 , C07D401/12 , C07D405/12 , C07D413/12 , C07D417/12
摘要： The present invention provides compounds of formula (I), wherein R1 is a monocyclic 5- or 6-membered heteroaryl; R4 is phenyl or monocyclic 5- or 6-membered heteroaryl; and the other substituents as defined in the claims, that inhibit cell and cell division and that inhibit the activation of Hypoxia Inducible Factor (HIF)—mediated transcription and signaling under hypoxic conditions. In one aspect, the compounds of the present invention are useful for the preparation of a medicament for the treatment or prevention of a disease or disorder selected from the group consisting of an inflammatory disease, a hyperproliferative disease or disorder, a hypoxia-related pathology and a disease characterized by excessive vascularisation. Also provided is a pharmaceutical composition, comprising a compound of the invention and a second therapeutic agent or radiation, useful for the treatment or prevention of the mentioned diseases or disorders.
摘要翻译：本发明提供式（I）化合物，其中R 1是单环的5或6元杂芳基; R4是苯基或单环的5或6元杂芳基; 和权利要求中定义的其它取代基，其在缺氧条件下抑制细胞和细胞分裂并抑制缺氧诱导因子（HIF）介导的转录和信号传导的活化。一方面，本发明的化合物可用于制备用于治疗或预防选自以下的疾病或病症的药物：炎性疾病，过度增殖性疾病或病症，缺氧相关病理学和一种以血管过度为特征的疾病。还提供了一种药物组合物，其包含可用于治疗或预防所述疾病或病症的本发明化合物和第二治疗剂或辐射。

3. 发明申请

US20100099843A1 DOLASTATIN 15 DERIVATIVES 有权
标题翻译： DOLASTATIN 15衍生物
公开(公告)号：US20100099843A1
公开(公告)日：2010-04-22
申请号：US12648446
申请日：2009-12-29
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： C07K5/037
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）和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，对 - 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。

4. 发明授权

US06248865B1 Compounds useful for the synthesis of dolastatin analogs 有权
标题翻译：可用于合成多拉司他汀类似物的化合物
公开(公告)号：US06248865B1
公开(公告)日：2001-06-19
申请号：US09211013
申请日：1998-12-15
申请人： Wilhelm Amberg , Harald Bernard , Ernst Buschmann , Andreas Haupt , Lothar Janitschke , Bernd Janssen , Ulrich Karl , Andreas Kling , Stefan Müller , Bernd de Potzolli , Kurt Ritter , Marco Thyes , Thomas Zierke
发明人： Wilhelm Amberg , Harald Bernard , Ernst Buschmann , Andreas Haupt , Lothar Janitschke , Bernd Janssen , Ulrich Karl , Andreas Kling , Stefan Müller , Bernd de Potzolli , Kurt Ritter , Marco Thyes , Thomas Zierke
IPC分类号： C07K700
CPC分类号： C07K7/06 , C07K5/101
摘要： Compounds of the formula where R1, R2, R3 and R4 have the meaning stated in the description, and a process for preparing them are described. The compounds are suitable as starting material for synthesizing substances which are active against tumors.
摘要翻译：制备方法R1，R2，R3和R4的化合物具有说明书中所述的含义，并描述了制备它们的方法。该化合物适用于合成对肿瘤有活性的物质的起始原料。

5. 发明授权

US6143721A Dolastatin 15 derivatives 失效
标题翻译： Dolastatin 15衍生物
公开(公告)号：US6143721A
公开(公告)日：2000-11-07
申请号：US896394
申请日：1997-07-18
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： A61K38/00 , A61K38/08 , A61P35/00 , C07K7/06 , C12P19/34
CPC分类号： C07K7/06 , C12P19/34 , A61K38/00
摘要： Compounds of the present invention include cell growth inhibitors which are peptides of Formula I,A-B-D-E-F-(G).sub.r -(K).sub.s -L (I),and acid salts thereof, wherein A, B, D, E, F, G and K are .alpha.-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 .beta.-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。

6. 发明授权

US5965700A Preparation of active peptides 失效
标题翻译：活性肽的制备
公开(公告)号：US5965700A
公开(公告)日：1999-10-12
申请号：US983460
申请日：1998-01-13
申请人： Wilhelm Amberg , Harald Bernard , Ernst Buschmann , Andreas Haupt , Bernd Janssen , Ulrich Karl , Andreas Kling , Stefan Muller , Kurt Ritter , Thomas Zierke
发明人： Wilhelm Amberg , Harald Bernard , Ernst Buschmann , Andreas Haupt , Bernd Janssen , Ulrich Karl , Andreas Kling , Stefan Muller , Kurt Ritter , Thomas Zierke
IPC分类号： C07K1/02 , C07K1/12 , C07K5/078 , C07K5/083 , C07K5/103 , C07K7/06 , A61K38/08
CPC分类号： C07K7/06 , C07K5/06165 , C07K5/0808 , C07K5/101
摘要： A process for preparing pentapeptides of the formula I ##STR1## where A and R.sup.1 -R.sup.3 have the stated meanings, comprises assembling the pentapeptide stepwise starting from a prolinamide of the formula II ##STR2## where R.sup.1 and R.sup.2 have the abovementioned meanings, and eliminating the group --NR.sup.1 R.sup.2 by hydrolysis where appropriate the peptide obtained in this way.
摘要翻译： PCT No.PCT / EP96 / 03073。 371日期1998年1月13日 102（e）1998年1月13日PCT PCT 1996年7月12日PCT公布。公开号WO97 / 05162 日期1997年2月13日一种制备式I的五肽的方法，其中A和R 1 -R 3具有所述含义，包括从式II的脯氨酸酰胺逐步组装五肽，其中R1和R2具有上述含义，基团-NR1R2通过水解合适地以这种方式获得的肽。

7. 发明授权

US5939527A Tetrapeptides as antitumor agents 失效
标题翻译：四肽作为抗肿瘤剂
公开(公告)号：US5939527A
公开(公告)日：1999-08-17
申请号：US688335
申请日：1996-07-30
申请人： Teresa Barlozzari , Andreas Haupt , Bernd Janssen , Christian Griesinger , Daniel Belik , Michael Boretzky
发明人： Teresa Barlozzari , Andreas Haupt , Bernd Janssen , Christian Griesinger , Daniel Belik , Michael Boretzky
IPC分类号： A61K38/00 , A61P35/00 , C07K4/00 , C07K5/02 , C07K5/00
CPC分类号： C07K5/0205 , A61K38/00
摘要： The present invention provides anti-tumor peptides of Formula I,A--B--NR.sup.3 --CHD--CH(OCH.sub.3)--CH.sub.2 CO--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 R.sup.1 R.sup.2 N--CHX--CO, wherein R.sup.1 is a-methyl group or an ethyl group, R.sup.2 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.sup.3 is a hydrogen atom or a methyl group. D is a normal or branched C.sub.2 -C.sub.5 -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.
摘要翻译：本发明提供式I，A-B-NR3-CHD-CH（OCH3）-CH2CO-E-K（I）的抗肿瘤肽及其酸式盐。 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 R 2 N-CHX-的氨基酸残基的氨基酸残基， CO，其中R1是α-甲基或乙基，R2是氢原子，甲基或乙基，X是烷基。 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。 R3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，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。

8. 发明授权

US5741892A Pentapeptides as antitumor agents 失效
标题翻译：五肽作为抗肿瘤剂
公开(公告)号：US5741892A
公开(公告)日：1998-04-21
申请号：US688334
申请日：1996-07-30
申请人： Teresa Barlozzari , Andreas Haupt , Bernd Janssen , Christian Griesinger , Daniel Belik , Michael Boretzky , George R. Pettit
发明人： Teresa Barlozzari , Andreas Haupt , Bernd Janssen , Christian Griesinger , Daniel Belik , Michael Boretzky , George R. Pettit
IPC分类号： A61K38/00 , A61P1/00 , A61P11/00 , A61P15/00 , A61P35/00 , C07K7/02 , C07K7/00
CPC分类号： C07K7/02 , A61K38/00
摘要： The present invention provides anti-tumor peptides of Formula I, A-B-N (CH.sub.3)-CHD-CH(OCH.sub.3)-CH.sub.2 CO-Pro-Pro-K (I), and the acid salts thereof. A is an amino acid residue of the formula (CH.sub.3).sub.2 N--CHX--CO, wherein X is a normal or branched alkyl group. B is an amino acid residue selected from the group consisting of valyl, isoleucyl, leucyl, and 2-t-butylglycyl. D is a normal or branched C.sub.3 -C.sub.4 -alkyl group. K is a t-butoxy group or a substituted 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.
摘要翻译：本发明提供式I，A-B-N（CH 3）-CHD-CH（OCH 3）-CH 2 CO-Pro-Pro-K（I）的抗肿瘤肽及其酸式盐。 A是式（CH 3）2 N-CHX-CO的氨基酸残基，其中X是正或支链烷基。 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。 D是正链或支链C 3 -C 4 - 烷基。 K为叔丁氧基或取代氨基。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，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。

9. 发明授权

US5527945A Diphenylheteroalkyl derivatives, the preparation thereof and drugs and cosmetics prepared therefrom 失效
标题翻译：二苯基杂烷基衍生物，其制备方法和由其制备的药物和化妆品
公开(公告)号：US5527945A
公开(公告)日：1996-06-18
申请号：US297537
申请日：1994-08-31
申请人： Bernd Janssen , Hans-Heiner Wuest
发明人： Bernd Janssen , Hans-Heiner Wuest
IPC分类号： A61K8/33 , A61K8/34 , A61K8/36 , A61K8/37 , A61K8/40 , A61K8/41 , A61K8/42 , A61K8/44 , A61K8/46 , A61K8/67 , A61K31/195 , A61Q19/00 , C07C37/11 , C07C39/17 , C07C43/20 , C07C43/205 , C07C43/21 , C07C43/23 , C07C45/44 , C07C47/575 , C07C51/367 , C07C59/70 , C07C65/21 , C07C65/24 , C07C65/26 , C07C69/76 , C07C69/92 , C07C205/06 , C07C205/34 , C07C205/35 , C07C205/37 , C07C211/60 , C07C217/48 , C07C217/58 , C07C217/76 , C07C217/86 , C07C223/06 , C07C229/38 , C07C229/60 , C07C233/18 , C07C233/25 , C07C233/43 , C07C233/47 , C07C233/48 , C07C233/75 , C07C235/42 , C07C255/51 , C07C255/54 , C07C259/10 , C07C309/42 , C07C317/22 , C07C317/32 , C07C317/44 , C07C323/16 , C07C323/19 , C07C323/20 , C07C323/32 , C07C323/34 , C07C323/36 , C07C323/41 , C07C323/56 , C07C323/62 , C07C327/30 , C07D263/58 , C07D311/72 , C07F9/38 , C07F9/40 , C07C255/49 , A61K31/275 , C07C69/02
CPC分类号： A61K8/46 , A61K8/33 , A61K8/34 , A61K8/36 , A61K8/37 , A61K8/40 , A61K8/41 , A61K8/411 , A61K8/42 , A61K8/445 , A61K8/671 , A61Q19/00 , C07C205/06 , C07C205/34 , C07C205/35 , C07C205/37 , C07C211/60 , C07C217/48 , C07C217/58 , C07C217/76 , C07C217/86 , C07C223/06 , C07C229/38 , C07C229/60 , C07C233/18 , C07C233/25 , C07C233/43 , C07C233/47 , C07C233/48 , C07C233/75 , C07C235/42 , C07C255/54 , C07C259/10 , C07C309/42 , C07C317/22 , C07C317/32 , C07C317/44 , C07C323/16 , C07C323/19 , C07C323/20 , C07C323/32 , C07C323/34 , C07C323/36 , C07C323/41 , C07C323/56 , C07C323/62 , C07C327/30 , C07C37/18 , C07C39/17 , C07C41/26 , C07C43/202 , C07C43/2055 , C07C43/21 , C07C43/23 , C07C45/44 , C07C47/575 , C07C51/367 , C07C65/24 , C07C65/26 , C07C69/76 , C07C69/92 , C07D263/58 , C07D311/58 , C07D311/70 , C07D311/72 , C07D317/22 , C07F9/3834 , C07F9/4021 , C07C2102/10
摘要： Diphenylheteroalkyl derivatives of the formula I ##STR1## where A and R.sup.1 -R.sup.6 have the meanings specified in the description, and the preparation thereof are described.The substances are suitable for controlling diseases and as cosmetic agents.
摘要翻译：描述了其中A和R 1 -R 6具有说明书中规定的含义的式I的（I）的二苯基杂烷基衍生物及其制备。该物质适用于控制疾病和化妆品。

10. 发明授权

US5248823A Diphenylheteroalkyl derivatives, the preparation thereof and drugs and cosmetics prepared therefrom 失效
标题翻译：二苯基杂烷基衍生物，其制备方法和由其制备的药物和化妆品
公开(公告)号：US5248823A
公开(公告)日：1993-09-28
申请号：US985934
申请日：1992-12-04
申请人： Bernd Janssen , Hans-Heiner Wuest
发明人： Bernd Janssen , Hans-Heiner Wuest
IPC分类号： A61K8/33 , A61K8/34 , A61K8/36 , A61K8/37 , A61K8/40 , A61K8/41 , A61K8/42 , A61K8/44 , A61K8/46 , A61Q19/00 , C07C39/17 , C07C43/20 , C07C43/205 , C07C43/21 , C07C43/23 , C07C45/44 , C07C47/575 , C07C65/24 , C07C65/26 , C07C69/76 , C07C69/92 , C07C205/06 , C07C205/34 , C07C205/37 , C07C211/60 , C07C217/48 , C07C217/58 , C07C217/76 , C07C217/86 , C07C223/06 , C07C229/38 , C07C229/60 , C07C233/18 , C07C233/25 , C07C233/43 , C07C233/47 , C07C233/48 , C07C233/75 , C07C235/42 , C07C235/46 , C07C255/54 , C07C259/10 , C07C309/42 , C07C317/22 , C07C317/44 , C07C323/16 , C07C323/20 , C07C323/32 , C07C323/41 , C07C323/56 , C07C323/62 , C07D311/72 , C07F9/38 , C07F9/40
CPC分类号： C07F9/3834 , A61K8/33 , A61K8/34 , A61K8/36 , A61K8/37 , A61K8/40 , A61K8/41 , A61K8/411 , A61K8/42 , A61K8/445 , A61K8/46 , A61Q19/00 , C07C205/06 , C07C205/34 , C07C205/37 , C07C211/60 , C07C217/48 , C07C217/58 , C07C217/76 , C07C217/86 , C07C223/06 , C07C229/38 , C07C229/60 , C07C233/18 , C07C233/25 , C07C233/43 , C07C233/47 , C07C233/48 , C07C233/75 , C07C235/42 , C07C255/54 , C07C259/10 , C07C309/42 , C07C317/22 , C07C317/44 , C07C323/16 , C07C323/20 , C07C323/32 , C07C323/41 , C07C323/56 , C07C323/62 , C07C39/17 , C07C43/202 , C07C43/2055 , C07C43/21 , C07C43/23 , C07C45/44 , C07C47/575 , C07C65/24 , C07C65/26 , C07C69/76 , C07C69/92 , C07D311/72 , C07F9/4021 , C07C2102/10
摘要： Diphenylheteroalkyl derivatives of the formula I ##STR1## where A and R.sup.1 -R.sup.6 have the meanings specified in the description, and the preparation thereof are described.The substances are suitable for controlling diseases and as cosmetic agents.
摘要翻译：描述了其中A和R 1 -R 6具有说明书中规定的含义的式I的（I）的二苯基杂烷基衍生物及其制备。该物质适用于控制疾病和化妆品。

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