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公开(公告)号:US20140228405A1
公开(公告)日:2014-08-14
申请号:US14237440
申请日:2012-08-08
申请人: Naoki Tomita , Shigeo Kajii , Douglas Robert Cary , Daisuke Tomita , Shinichi Imamura , Ken Tsuchida , Satoru Matsuda , Ryujiro Hara
发明人: Naoki Tomita , Shigeo Kajii , Douglas Robert Cary , Daisuke Tomita , Shinichi Imamura , Ken Tsuchida , Satoru Matsuda , Ryujiro Hara
IPC分类号: C07C233/80 , C07D231/14 , C07D335/02 , C07D211/98
CPC分类号: C07C233/80 , A61K31/167 , A61K31/36 , A61K31/366 , A61K31/381 , A61K31/40 , A61K31/402 , A61K31/4035 , A61K31/404 , A61K31/4184 , A61K31/42 , A61K31/421 , A61K31/426 , A61K31/428 , A61K31/429 , A61K31/433 , A61K31/4406 , A61K31/4409 , A61K31/4453 , A61K31/4468 , A61K31/451 , A61K31/495 , A61K31/55 , C07C235/56 , C07C237/40 , C07C237/42 , C07C271/20 , C07C271/22 , C07C2601/02 , C07C2601/18 , C07C2602/08 , C07D207/06 , C07D207/337 , C07D209/08 , C07D209/42 , C07D209/46 , C07D209/48 , C07D211/40 , C07D211/56 , C07D211/58 , C07D211/76 , C07D211/98 , C07D213/04 , C07D213/38 , C07D213/56 , C07D223/16 , C07D231/14 , C07D231/20 , C07D231/22 , C07D231/26 , C07D231/56 , C07D233/61 , C07D233/64 , C07D239/36 , C07D261/08 , C07D261/10 , C07D263/32 , C07D263/34 , C07D277/20 , C07D277/28 , C07D277/30 , C07D277/62 , C07D285/06 , C07D295/135 , C07D295/14 , C07D295/155 , C07D309/14 , C07D317/58 , C07D333/20 , C07D335/02 , C07D405/04 , C07D409/04 , C07D471/04 , C07D495/04 , C07D513/04
摘要: The present invention provides a compound having a lysine-specific demethylase 1 inhibitory action, and useful as a medicament such as a prophylactic or therapeutic agent for cancer, and central nervous system diseases, and the like. The present invention relates to a compound represented by the formula wherein A is a hydrocarbon group or heterocyclic group optionally having substituent(s); R is H, a hydrocarbon group or heterocyclic group optionally having substituent(s); A and R are optionally bonded to each other to form a ring optionally having substituent(s); Q1, Q2, Q3 and Q4 are each a hydrogen atom or a substituent; Q1 and Q2, and Q3 and Q4, are each optionally bonded to each other to form a ring optionally having substituent(s); X is H, an acyclic hydrocarbon group or saturated cyclic group optionally having substituent(s); Y1, Y2 and Y3 are each H, a hydrocarbon group or heterocyclic group optionally having substituent(s); X and Y1, and Y1 and Y2, are each optionally bonded to each other to form a ring optionally having substituent(s); and Z1, Z2 and Z3 are each H or a substituent, or a salt thereof.
摘要翻译: 本发明提供具有赖氨酸特异性脱甲基酶1抑制作用的化合物,可用作癌症用预防或治疗剂等中药物等中药用药物。 本发明涉及由下式表示的化合物:其中A是任选具有取代基的烃基或杂环基; R是H,任选具有取代基的烃基或杂环基; A和R可以任选地彼此键合形成任选具有取代基的环; Q1,Q2,Q3和Q4各自为氢原子或取代基; Q1和Q2以及Q3和Q4各自任选地彼此结合形成任选具有取代基的环; X是H,任选具有取代基的无环烃基或饱和环基; Y 1,Y 2和Y 3各自为H,任选具有取代基的烃基或杂环基; X和Y1以及Y 1和Y 2各自任选地彼此键合以形成任选具有取代基的环; 并且Z 1,Z 2和Z 3各自为H或取代基,或其盐。
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公开(公告)号:US20100168424A1
公开(公告)日:2010-07-01
申请号:US12263841
申请日:2008-11-03
申请人: Nozomu SAKAI , Shinichi IMAMURA
发明人: Nozomu SAKAI , Shinichi IMAMURA
IPC分类号: C07D487/04
CPC分类号: C07D487/04
摘要: The present invention provides a fused heterocyclic derivative having a potent kinase inhibitory activity and use thereofA compound represented by the formula (I): wherein each symbol is as defined in the specification, except a particular compound, or a salt thereof, and a pharmaceutical agent containing the compound or a prodrug thereof, which is a kinase (VEGFR, VEGFR2, PDGFR, Raf) inhibitor, an angiogenesis inhibitor, an agent for the prophylaxis or treatment of cancer, a cancer growth inhibitor or a cancer metastasis suppressor.
摘要翻译: 本发明提供具有强激酶抑制活性的稠合杂环衍生物及其用途由式(I)表示的化合物:其中每个符号如说明书中所定义,除了特定化合物或其盐和药物 含有作为激酶(VEGFR,VEGFR2,PDGFR,Raf)抑制剂,血管发生抑制剂,癌症预防或治疗剂,癌症生长抑制剂或癌症转移抑制剂的化合物或其前药的药剂。
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公开(公告)号:US06562978B1
公开(公告)日:2003-05-13
申请号:US10089374
申请日:2002-03-29
申请人: Shinichi Imamura , Shohei Hashiguchi , Taeko Hattori , Osamu Nishimura , Naoyuki Kanzaki , Masanori Baba , Yoshihiro Sugihara
发明人: Shinichi Imamura , Shohei Hashiguchi , Taeko Hattori , Osamu Nishimura , Naoyuki Kanzaki , Masanori Baba , Yoshihiro Sugihara
IPC分类号: C07D21128
CPC分类号: C07D401/12 , C07D211/58 , C07D211/62 , C07D401/14 , C07D405/14 , C07D409/14 , C07D413/14 , C07D417/14 , C07D471/04 , C07D487/14
摘要: A compound of formula (I) (wherein R1 is a hydrogen atom, a hydrocarbon group which may be substituted, a non-aromatic heterocyclic group which may be substituted, R2 is a hydrocarbon group which may be substituted, a non-aromatic heterocyclic group which may be substituted, or R1 and R2 may combine to each other together with A to form a heterocyclic group which may be substituted; A is N or N+—R5.Y−(R5 is a hydrocarbon group; Y− is a counter anion); R3 is a cyclic hydrocarbon group which may be substituted or a heterocyclic group which may be substituted; n is 0 or 1; R4 is a hydrogen atom, a hydrocarbon group which may be substituted, a heterocyclic group which may be substituted, an alkoxy group which may be substituted, an aryloxy group which may be substituted, or an amino group which may be substituted, E is a divalent aliphatic hydrocarbon group which may be substituted by group(s) other than oxo; G1 is a bond, CO or SO2; G2 is CO, SO2, NHCO, CONH or OCO; J is methine or a nitrogen atom; and each of Q and R is a bond or a divalent C1-3 aliphatic hydrocarbon which may be substituted; provided that J is methine when G2 is OCO, that one of Q and R is not a bond when the other is a bond and that each of Q and R is not substituted by oxo group(s) when G1 is a bond) or a salt thereof has a potent CCR5 antagonistic activity and can be advantageously used for the treatment or prevention of infectious disease of various HIV in human (e.g. AIDS).
摘要翻译: 式(I)的化合物(其中R 1为氢原子,可被取代的烃基,可被取代的非芳族杂环基,R 2为可被取代的烃基,非芳香族杂环基 或者R 1和R 2可以与A相互结合形成可被取代的杂环基; A是N或-N + -R 5 .Y-(R 5是烃基; Y-是抗衡阴离子 ); R3是可以被取代的环状烃基或可以被取代的杂环基; n是0或1; R4是氢原子,可以被取代的烃基,可以被取代的杂环基, 可被取代的烷氧基,可被取代的芳氧基或可被取代的氨基,E是可被除氧以外的基团取代的二价脂族烃基; G 1是键,CO 或SO 2; G2是CO,SO 2,NHCO,CONH或OCO; J是次甲基或硝基 原子 Q和R分别为可以被取代的键或二价C 1-3脂族烃; 条件是当G2是OCO时J是次甲基,当另一个是键时Q和R中的一个不是键,并且当G 1是键时,Q和R各自不被氧代基取代)或 其盐具有有效的CCR5拮抗活性,可有利地用于治疗或预防人类各种HIV感染性疾病(如艾滋病)。
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公开(公告)号:US08044049B2
公开(公告)日:2011-10-25
申请号:US12064903
申请日:2007-08-03
IPC分类号: C07D487/04 , A61K31/5025 , A61P35/00
CPC分类号: C07D487/04
摘要: The present invention provides a fused heterocyclic derivative having a potent kinase inhibitory activity and use thereof.A compound represented by the formula (I): wherein each symbol is as defined in the specification, except a particular compound, or a salt thereof, and a pharmaceutical agent containing the compound or a prodrug thereof, which is a kinase (VEGFR, VEGFR2, PDGFR, Raf) inhibitor, an angiogenesis inhibitor, an agent for the prophylaxis or treatment of cancer, a cancer growth inhibitor or a cancer metastasis suppressor.
摘要翻译: 本发明提供具有强激酶抑制活性的稠合杂环衍生物及其应用。 由式(I)表示的化合物:其中每个符号如说明书中所定义,除了特定化合物或其盐,以及含有作为激酶的化合物或其前药的药物(VEGFR,VEGFR2 ,PDGFR,Raf)抑制剂,血管发生抑制剂,用于预防或治疗癌症的药物,癌症生长抑制剂或癌症转移抑制剂。
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公开(公告)号:US20090163488A1
公开(公告)日:2009-06-25
申请号:US12133063
申请日:2008-06-04
IPC分类号: A61K31/5377 , C07D471/04 , A61K31/437 , A61P35/04 , C07D495/04 , A61K31/496
CPC分类号: C07D471/04 , C07D417/12 , C07D471/14 , C07D513/04
摘要: A compound represented by the formula (I): wherein Z1, Z2, Z3 and Z4 are the following combination, (Z1,Z2,Z3,Z4)=(CR4,N,CR5,C), (N,N,CR5,C), (N,C,CR5,N), (S,C,CR5,C) or (S,C,N,C); R1 and R2 are the same or different and each is (1) a hydrogen atom, (2) a halogen atom, (3) a group bonded via a carbon atom, (4) a group bonded via a nitrogen atom, (5) a group bonded via an oxygen atom or (6) a group bonded via a sulfur atom; R3 is an amino optionally having substituent(s); R4 and R5 are the same or different and each is (1) a hydrogen atom, (2) a halogen atom, (3) a group bonded via a carbon atom, (4) a group bonded via a nitrogen atom, (5) a group bonded via an oxygen atom or (6) a group bonded via a sulfur atom; R3 and R4 optionally form a ring optionally having substituent(s); and a group represented by the formula is a cyclic group optionally having substituent(s), or a salt thereof.
摘要翻译: 由式(I)表示的化合物:其中Z 1,Z 2,Z 3和Z 4是以下组合:(Z 1,Z 2,Z 3,Z 4)=(CR 4,N,CR 5,C),(N,N, C),(N,C,CR5,N),(S,C,CR5,C)或(S,C,N,C) R1和R2相同或不同,分别为(1)氢原子,(2)卤素原子,(3)通过碳原子键合的基团,(4)通过氮原子键合的基团,(5) 通过氧原子键合的基团或(6)通过硫原子键合的基团; R3是任选具有取代基的氨基; R4和R5相同或不同,分别为(1)氢原子,(2)卤素原子,(3)通过碳原子键合的基团,(4)通过氮原子键合的基团,(5) 通过氧原子键合的基团或(6)通过硫原子键合的基团; R3和R4任选地形成任选具有取代基的环; 并且由下式表示的基团是任选具有取代基的环状基团或其盐。
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公开(公告)号:US20090137595A1
公开(公告)日:2009-05-28
申请号:US12064903
申请日:2007-08-03
IPC分类号: A61K31/5025 , C07D487/04
CPC分类号: C07D487/04
摘要: The present invention provides a fused heterocyclic derivative having a potent kinase inhibitory activity and use thereof.A compound represented by the formula (I): wherein each symbol is as defined in the specification, except a particular compound, or a salt thereof, and a pharmaceutical agent containing the compound or a prodrug thereof, which is a kinase (VEGFR, VEGFR2, PDGFR, Raf) inhibitor, an angiogenesis inhibitor, an agent for the prophylaxis or treatment of cancer, a cancer growth inhibitor or a cancer metastasis suppressor.
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公开(公告)号:US06174877B1
公开(公告)日:2001-01-16
申请号:US09101470
申请日:1998-07-10
申请人: Yukio Ishibashi , Shinichi Imamura , Tetsuo Miwa
发明人: Yukio Ishibashi , Shinichi Imamura , Tetsuo Miwa
IPC分类号: A61K3140
CPC分类号: C07D477/20
摘要: A cephem compound of the formula: wherein R1 stands for an optionally substituted lower alkyl group, R2 stands for H or a lower alkyl group, R3 stands for H, an optionally substituted hydrocarbon group, cyano group, a lower alkyloxy group or a lower alkylthio group, and the ring A stands for an optionally substituted non-quaternarized nitrogen-containing heterocyclic ring, provided that, when A is unsubstituted 2-pyridyl group, R3 stands for a group other than hydrogen, or their esters or salts, has excellent antibacterial activities, oral absorbability and stability, and is useful as an antibacterial agent.
摘要翻译: 下式的头孢烯化合物:其中R1代表任意取代的低级烷基,R2代表H或低级烷基,R3代表H,任意取代的烃基,氰基,低级烷氧基或低级烷硫基 并且环A代表任选取代的非季铵化含氮杂环,条件是当A是未取代的2-吡啶基时,R 3代表氢以外的基团或其酯或盐,具有优异的抗菌性 活性,口服吸收性和稳定性,可用作抗菌剂。
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公开(公告)号:US09278931B2
公开(公告)日:2016-03-08
申请号:US14237440
申请日:2012-08-08
申请人: Naoki Tomita , Shigeo Kajii , Douglas Robert Cary , Daisuke Tomita , Shinichi Imamura , Ken Tsuchida , Satoru Matsuda , Ryujiro Hara , Yusuke Tominari
发明人: Naoki Tomita , Shigeo Kajii , Douglas Robert Cary , Daisuke Tomita , Shinichi Imamura , Ken Tsuchida , Satoru Matsuda , Ryujiro Hara , Yusuke Tominari
IPC分类号: A61K31/167 , A61K31/435 , A61K31/415 , A61K31/382 , C07D295/14 , C07D231/14 , C07D231/56 , C07D231/20 , C07D231/22 , C07C233/80 , C07C271/22 , C07C235/56 , C07C237/40 , C07D211/98 , A61K31/36 , A61K31/366 , A61K31/381 , A61K31/40 , A61K31/402 , A61K31/4035 , A61K31/404 , A61K31/4184 , A61K31/42 , A61K31/421 , A61K31/426 , A61K31/428 , A61K31/429 , A61K31/433 , A61K31/4406 , A61K31/4409 , A61K31/4453 , A61K31/4468 , A61K31/451 , A61K31/495 , A61K31/55 , C07D309/14 , C07D317/58 , C07D223/16 , C07D333/20 , C07D233/61 , C07D233/64 , C07D405/04 , C07D239/36 , C07D409/04 , C07D471/04 , C07D261/08 , C07D261/10 , C07D263/32 , C07D263/34 , C07D207/06 , C07D495/04 , C07D207/337 , C07D277/20 , C07D277/28 , C07D277/30 , C07D209/08 , C07D277/62 , C07D209/42 , C07D513/04 , C07D209/46 , C07D209/48 , C07D285/06 , C07D211/56 , C07D211/58 , C07D211/76 , C07D213/04 , C07D213/38 , C07D213/56 , C07D335/02
CPC分类号: C07C233/80 , A61K31/167 , A61K31/36 , A61K31/366 , A61K31/381 , A61K31/40 , A61K31/402 , A61K31/4035 , A61K31/404 , A61K31/4184 , A61K31/42 , A61K31/421 , A61K31/426 , A61K31/428 , A61K31/429 , A61K31/433 , A61K31/4406 , A61K31/4409 , A61K31/4453 , A61K31/4468 , A61K31/451 , A61K31/495 , A61K31/55 , C07C235/56 , C07C237/40 , C07C237/42 , C07C271/20 , C07C271/22 , C07C2601/02 , C07C2601/18 , C07C2602/08 , C07D207/06 , C07D207/337 , C07D209/08 , C07D209/42 , C07D209/46 , C07D209/48 , C07D211/40 , C07D211/56 , C07D211/58 , C07D211/76 , C07D211/98 , C07D213/04 , C07D213/38 , C07D213/56 , C07D223/16 , C07D231/14 , C07D231/20 , C07D231/22 , C07D231/26 , C07D231/56 , C07D233/61 , C07D233/64 , C07D239/36 , C07D261/08 , C07D261/10 , C07D263/32 , C07D263/34 , C07D277/20 , C07D277/28 , C07D277/30 , C07D277/62 , C07D285/06 , C07D295/135 , C07D295/14 , C07D295/155 , C07D309/14 , C07D317/58 , C07D333/20 , C07D335/02 , C07D405/04 , C07D409/04 , C07D471/04 , C07D495/04 , C07D513/04
摘要: The present invention provides a compound having a lysine-specific demethylase 1 inhibitory action, and useful as a medicament such as a prophylactic or therapeutic agent for cancer, and central nervous system diseases, and the like. The present invention relates to a compound represented by the formula wherein A is a hydrocarbon group or heterocyclic group optionally having substituent(s); R is H, a hydrocarbon group or heterocyclic group optionally having substituent(s); A and R are optionally bonded to each other to form a ring optionally having substituent(s); Q1, Q2, Q3 and Q4 are each a hydrogen atom or a substituent; Q1 and Q2, and Q3 and Q4, are each optionally bonded to each other to form a ring optionally having substituent(s); X is H, an acyclic hydrocarbon group or saturated cyclic group optionally having substituent(s); Y1, Y2 and Y3 are each H, a hydrocarbon group or heterocyclic group optionally having substituent(s); X and Y1, and Y1 and Y2, are each optionally bonded to each other to form a ring optionally having substituent(s); and Z1, Z2 and Z3 are each H or a substituent, or a salt thereof.
摘要翻译: 本发明提供具有赖氨酸特异性脱甲基酶1抑制作用的化合物,可用作癌症用预防或治疗剂等中药物等中药用药物。 本发明涉及由下式表示的化合物:其中A是任选具有取代基的烃基或杂环基; R是H,任选具有取代基的烃基或杂环基; A和R可以任选地彼此键合形成任选具有取代基的环; Q1,Q2,Q3和Q4各自为氢原子或取代基; Q1和Q2以及Q3和Q4各自任选地彼此结合形成任选具有取代基的环; X是H,任选具有取代基的无环烃基或饱和环基; Y 1,Y 2和Y 3各自为H,任选具有取代基的烃基或杂环基; X和Y1以及Y 1和Y 2各自任选地彼此键合以形成任选具有取代基的环; 并且Z 1,Z 2和Z 3各自为H或取代基,或其盐。
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公开(公告)号:US08772277B2
公开(公告)日:2014-07-08
申请号:US13566091
申请日:2012-08-03
申请人: Shigemitsu Matsumoto , Koji Ono , Yusuke Tominari , Taisuke Katoh , Kazuhiro Miwa , Atsushi Hasuoka , Shinichi Imamura
发明人: Shigemitsu Matsumoto , Koji Ono , Yusuke Tominari , Taisuke Katoh , Kazuhiro Miwa , Atsushi Hasuoka , Shinichi Imamura
IPC分类号: A61K31/00 , C07D401/00
CPC分类号: C07D417/14 , C07D417/06 , C07D451/02
摘要: The present invention provides a novel compound having a superior activity as an ERR-α modulator and useful as an agent for the prophylaxis or treatment of ERR-α associated diseases.The present invention relates to a compound represented by the formula wherein each symbol is as defined in the specification, or a salt thereof.
摘要翻译: 本发明提供作为ERR-α调节剂具有优异活性的新型化合物,可用作预防或治疗ERR-α相关疾病的药剂。 本发明涉及由下式表示的化合物,其中每个符号如说明书中所定义,或其盐。
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公开(公告)号:US20130072467A1
公开(公告)日:2013-03-21
申请号:US13566091
申请日:2012-08-03
申请人: Shigemitsu MATSUMOTO , Koji Ono , Yusuke Tominari , Taisuke Katoh , Kazuhiro Miwa , Atsushi Hasuoka , Shinichi Imamura
发明人: Shigemitsu MATSUMOTO , Koji Ono , Yusuke Tominari , Taisuke Katoh , Kazuhiro Miwa , Atsushi Hasuoka , Shinichi Imamura
IPC分类号: C07D417/14 , A61K31/519 , C07D417/06 , C07D513/04 , A61K31/429
CPC分类号: C07D417/14 , C07D417/06 , C07D451/02
摘要: The present invention provides a novel compound having a superior activity as an ERR-α modulator and useful as an agent for the prophylaxis or treatment of ERR-α associated diseases.The present invention relates to a compound represented by the formula wherein each symbol is as defined in the specification, or a salt thereof.
摘要翻译: 本发明提供作为ERR-α调节剂具有优异活性的新型化合物,可用作预防或治疗ERR-α相关疾病的药剂。 本发明涉及由下式表示的化合物,其中每个符号如说明书中所定义,或其盐。
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