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1. 发明授权

US08791263B2 Cortistatin A analog and use thereof 有权
标题翻译：皮质他汀类似物及其用途
公开(公告)号：US08791263B2
公开(公告)日：2014-07-29
申请号：US13823265
申请日：2011-09-16
申请人： Motomasa Kobayashi , Naoyuki Kotoku , Masayoshi Arai , Satoru Tamura
发明人： Motomasa Kobayashi , Naoyuki Kotoku , Masayoshi Arai , Satoru Tamura
IPC分类号： C07D405/04 , C07D217/02 , A61K45/00 , A61K31/4725 , A61P43/00 , A61P35/00 , C07D407/10 , C07F7/18 , A61K45/06
CPC分类号： C07D407/10 , A61K31/4725 , A61K45/06 , C07D405/04 , C07F7/1804
摘要： A compound represented by the general formula (M): (wherein R1 represents a substituted or unsubstituted aromatic heterocyclic group, R2 represents a hydrogen atom, a substituted or unsubstituted alkyl group having 1 to 3 carbon atoms, OR3, N(R3)2, C(═O)OR3 or C(═O)N(R3)2, R3 represents a hydrogen atom, an alkyl group having 1 to 4 carbon atoms, or an acyl group having 1 to 4 carbon atoms, R4 represents a hydrogen atom, an oxygen atom or OR5, and R5 represents a hydrogen atom, an alkyl group having 1 to 3 carbon atoms, or an acyl group having 1 to 3 carbon atoms); or a pharmaceutically acceptable salt thereof is a cortistatin A analog which is useful as an active ingredient of medicaments for cancer prevention or treatment in that the analog can be mass-produced by chemical synthesis due to its simple chemical structure and retains the same biological activities as those of cortistatin A.
摘要翻译：由通式（M）表示的化合物：其中，R1表示取代或未取代的芳香族杂环基，R2表示氢原子，取代或未取代的碳原子数1〜3的烷基，OR3，N（R3）2， C（= O）OR 3或C（= O）N（R3）2，R3表示氢原子，碳原子数1〜4的烷基或碳原子数1〜4的酰基，R4表示氢原子，氧原子或OR 5，R5表示氢原子，碳原子数1〜3的烷基或碳原子数1〜3的酰基）。或其药学上可接受的盐是可用作癌症预防或治疗药物的活性成分的皮质激素A类似物，因为类似物可以通过化学合成由于其简单的化学结构而大规模生产，并保持与皮质激素A.

2. 发明申请

US20130065937A1 NOVEL PRENYLARENE COMPOUND AND USE THEREOF 有权
标题翻译：新颖的苯乙烯化合物及其用途
公开(公告)号：US20130065937A1
公开(公告)日：2013-03-14
申请号：US13696425
申请日：2011-05-06
申请人： Motomasa Kobayashi , Naoyuki Kotoku , Masayoshi Arai , Takashi Kawachi
发明人： Motomasa Kobayashi , Naoyuki Kotoku , Masayoshi Arai , Takashi Kawachi
IPC分类号： C07D333/08 , A61P35/00 , A61K31/341 , A61K31/381 , C07D307/36
CPC分类号： C07D307/36 , A61K31/341 , A61K31/381 , A61K45/06 , C07D333/08 , A61K2300/00
摘要： A compound represented by the general formula (C): (wherein R101 represents a substituted or unsubstituted aromatic heterocyclic group, R102, R103, R104 and R105 may be the same or different, and each represents a hydrogen atom, a halogen atom, an alkyl group having 1 to 3 carbon atoms, or a haloalkyl group having 1 to 3 carbon atoms, and R106 represents a hydrogen atom, or a saturated or unsaturated hydrocarbon group which is a straight or branched chain having 1 to 12 carbon atoms, but excluded is the case where R101 is a 3-furyl group, R102, R103, R104 and R105 are all methyl groups, and R106 is a methyl group, a 4-methyl-3-pentenyl group or a 4,8-dimethyl-3,7-nonadienyl group); or a pharmaceutically acceptable salt thereof has selective inhibitory activity on hypoxic cell growth in a broad range of the concentration and therefore is useful as an active ingredient of a medicament for cancer prevention or treatment.
摘要翻译：由通式（C）表示的化合物：（其中R 101表示取代或未取代的芳族杂环基，R 102，R 103，R 104和R 105可以相同或不同，表示氢原子，卤素原子，烷基具有1至3个碳原子的烷基或具有1至3个碳原子的卤代烷基，R 10 6表示氢原子，或具有1至12个碳原子的直链或支链的饱和或不饱和烃基，但不包括 R 101为3-呋喃基的情况，R102，R103，R104，R105均为甲基，R106为甲基，4-甲基-3-戊烯基或4,8-二甲基-3,7 - 壬二烯基）; 或其药学上可接受的盐在宽范围的浓度下对缺氧细胞生长具有选择性抑制活性，因此可用作用于癌症预防或治疗的药物的活性成分。

3. 发明授权

US09371301B2 Prenylarene compound and use thereof 有权
标题翻译：普萘酰芳烃化合物及其用途
公开(公告)号：US09371301B2
公开(公告)日：2016-06-21
申请号：US13696425
申请日：2011-05-06
申请人： Motomasa Kobayashi , Naoyuki Kotoku , Masayoshi Arai , Takashi Kawachi
发明人： Motomasa Kobayashi , Naoyuki Kotoku , Masayoshi Arai , Takashi Kawachi
IPC分类号： C07D307/36 , C07D333/06 , A61K31/341 , A61K31/381 , A61K45/06 , C07D333/08
CPC分类号： C07D307/36 , A61K31/341 , A61K31/381 , A61K45/06 , C07D333/08 , A61K2300/00
摘要： A compound represented by the general formula (C): (wherein R101 represents a substituted or unsubstituted aromatic heterocyclic group, R102, R103, R104 and R105 may be the same or different, and each represents a hydrogen atom, a halogen atom, an alkyl group having 1 to 3 carbon atoms, or a haloalkyl group having 1 to 3 carbon atoms, and R106 represents a hydrogen atom, or a saturated or unsaturated hydrocarbon group which is a straight or branched chain having 1 to 12 carbon atoms, but excluded is the case where R101 is a 3-furyl group, R102, R103, R104 and R105 are all methyl groups, and R106 is a methyl group, a 4-methyl-3-pentenyl group or a 4,8-dimethyl-3,7-nonadienyl group); or a pharmaceutically acceptable salt thereof has selective inhibitory activity on hypoxic cell growth in a broad range of the concentration and therefore is useful as an active ingredient of a medicament for cancer prevention or treatment.
摘要翻译：由通式（C）表示的化合物：（其中R 101表示取代或未取代的芳族杂环基，R 102，R 103，R 104和R 105可以相同或不同，表示氢原子，卤素原子，烷基具有1至3个碳原子的烷基或具有1至3个碳原子的卤代烷基，R 10 6表示氢原子，或具有1至12个碳原子的直链或支链的饱和或不饱和烃基，但不包括 R 101为3-呋喃基的情况，R102，R103，R104，R105均为甲基，R106为甲基，4-甲基-3-戊烯基或4,8-二甲基-3,7 - 壬二烯基）; 或其药学上可接受的盐在宽范围的浓度下对缺氧细胞生长具有选择性抑制活性，因此可用作用于癌症预防或治疗的药物的活性成分。

4. 发明申请

US20130210859A1 NOVEL CORTISTATIN A ANALOG AND USE THEREOF 有权
标题翻译：一个模拟和其使用的新的CORTISTATIN
公开(公告)号：US20130210859A1
公开(公告)日：2013-08-15
申请号：US13823265
申请日：2011-09-16
申请人： Motomasa Kobayashi , Naoyuki Kotoku , Masayoshi Arai , Satoru Tamura
发明人： Motomasa Kobayashi , Naoyuki Kotoku , Masayoshi Arai , Satoru Tamura
IPC分类号： C07D407/10
CPC分类号： C07D407/10 , A61K31/4725 , A61K45/06 , C07D405/04 , C07F7/1804
摘要： A compound represented by the general formula (M): (wherein R1 represents a substituted or unsubstituted aromatic heterocyclic group, R2 represents a hydrogen atom, a substituted or unsubstituted alkyl group having 1 to 3 carbon atoms, OR3, N(R3)2, C(═O)OR3 or C(═O)N(R3)2, R3 represents a hydrogen atom, an alkyl group having 1 to 4 carbon atoms, or an acyl group having 1 to 4 carbon atoms, R4 represents a hydrogen atom, an oxygen atom or OR5, and R5 represents a hydrogen atom, an alkyl group having 1 to 3 carbon atoms, or an acyl group having 1 to 3 carbon atoms); or a pharmaceutically acceptable salt thereof is a cortistatin A analog which is useful as an active ingredient of medicaments for cancer prevention or treatment in that the analog can be mass-produced by chemical synthesis due to its simple chemical structure and retains the same biological activities as those of cortistatin A.
摘要翻译：由通式（M）表示的化合物：其中，R1表示取代或未取代的芳香族杂环基，R2表示氢原子，取代或未取代的碳原子数1〜3的烷基，OR3，N（R3）2， C（= O）OR 3或C（= O）N（R 3）2，R 3表示氢原子，碳原子数1〜4的烷基或碳原子数1〜4的酰基，，氧原子或OR 5，R5表示氢原子，碳原子数1〜3的烷基或碳原子数1〜3的酰基）。或其药学上可接受的盐是可用作癌症预防或治疗药物的活性成分的皮质激素A类似物，因为类似物可以通过化学合成由于其简单的化学结构而大规模生产，并保持与皮质激素A.

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