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1. 发明授权

US08034812B2 Imidazopyridazine derivative having kinase inhibitory activity and pharmaceutical agent thereof 有权
标题翻译：具有激酶抑制活性的咪唑并哒嗪衍生物及其药剂
公开(公告)号：US08034812B2
公开(公告)日：2011-10-11
申请号：US12263884
申请日：2008-11-03
申请人： Nozomu Sakai , Shinichi Imamura , Naoki Miyamoto , Takaharu Hirayama
发明人： Nozomu Sakai , Shinichi Imamura , Naoki Miyamoto , Takaharu Hirayama
IPC分类号： C07D487/04 , A61K31/4985 , A61P35/00
CPC分类号： C07D487/04
摘要： The present invention provides an imidazopyridazine derivative compound having a potent kinase inhibitory activity and a pharmaceutical agent thereof useful for treatment or prevention of cancer and the like. One such compound is represented by the formula: or a salt thereof or a prodrug thereof. The pharmaceutical agent contains the imidazopyridazine derivative 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：本发明提供了可用于治疗或预防癌症等的具有强激酶抑制活性的咪唑并哒嗪衍生化合物及其药剂。一种这样的化合物由下式表示：或其盐或其前药。药剂含有作为激酶（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的咪唑并哒嗪衍生物化合物或其前药转移抑制因子

2. 发明授权

US08044049B2 Fused heterocyclic derivative and use thereof 有权
标题翻译：熔融杂环衍生物及其用途
公开(公告)号：US08044049B2
公开(公告)日：2011-10-25
申请号：US12064903
申请日：2007-08-03
申请人： Nozomu Sakai , Shinichi Imamura , Naoki Miyamoto , Takaharu Hirayama
发明人： Nozomu Sakai , Shinichi Imamura , Naoki Miyamoto , Takaharu Hirayama
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。

3. 发明申请

US20090137595A1 FUSED HETEROCYCLIC DERIVATIVE AND USE THEREOF 有权
公开(公告)号：US20090137595A1
公开(公告)日：2009-05-28
申请号：US12064903
申请日：2007-08-03
申请人： Nozomu Sakai , Shinichi Imamura , Naoki Miyamoto , Takaharu Hirayama
发明人： Nozomu Sakai , Shinichi Imamura , Naoki Miyamoto , Takaharu Hirayama
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.

4. 发明授权

US08273741B2 Imidazo-pyridazinyl compounds and uses thereof 有权
标题翻译：咪唑并哒嗪化合物及其用途
公开(公告)号：US08273741B2
公开(公告)日：2012-09-25
申请号：US12263949
申请日：2008-11-03
申请人： Nozomu Sakai , Shinichi Imamura , Naoki Miyamoto , Takaharu Hirayama
发明人： Nozomu Sakai , Shinichi Imamura , Naoki Miyamoto , Takaharu Hirayama
IPC分类号： C07D487/04 , A01N43/58 , 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。

5. 发明授权

US08445509B2 Fused heterocyclic derivatives and use thereof 失效
标题翻译：稠合杂环衍生物及其用途
公开(公告)号：US08445509B2
公开(公告)日：2013-05-21
申请号：US12990760
申请日：2009-05-07
申请人： Naoki Miyamoto , Shigemitsu Matsumoto , Shinichi Imamura
发明人： Naoki Miyamoto , Shigemitsu Matsumoto , Shinichi Imamura
IPC分类号： A61K31/44 , C07D491/02 , C07D498/02
CPC分类号： C07D513/04 , C07D277/82 , C07D471/04
摘要： The present invention provides a fused heterocyclic derivative having a strong kinase inhibitory activity and use thereof.The present invention relates to a compound represented by the formula wherein each symbol is as defined in the present specification, or a salt thereof.
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。本发明涉及由下式表示的化合物，其中每个符号如本说明书中所定义，或其盐。

6. 发明申请

US20110046169A1 FUSED HETEROCYCLIC DERIVATIVES AND USE THEREOF 失效
标题翻译：熔融杂环衍生物及其用途
公开(公告)号：US20110046169A1
公开(公告)日：2011-02-24
申请号：US12990760
申请日：2009-05-07
申请人： Naoki Miyamoto , Shigemitsu Matsumoto , Shinichi Imamura
发明人： Naoki Miyamoto , Shigemitsu Matsumoto , Shinichi Imamura
IPC分类号： A61K31/513 , C07D471/04 , C07D277/82 , C07D513/04 , A61K31/437 , A61K31/428 , A61P35/00
CPC分类号： C07D513/04 , C07D277/82 , C07D471/04
摘要： The present invention provides a fused heterocyclic derivative having a strong kinase inhibitory activity and use thereof.The present invention relates to a compound represented by the formula wherein each symbol is as defined in the present specification, or a salt thereof.
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。本发明涉及由下式表示的化合物，其中每个符号如本说明书中所定义，或其盐。

7. 发明授权

US07348324B2 Cyclic amine compounds as CCR5 antagonists 有权
标题翻译：环胺化合物作为CCR5拮抗剂
公开(公告)号：US07348324B2
公开(公告)日：2008-03-25
申请号：US10273111
申请日：2002-10-18
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： A61P31/18 , A61K31/535 , A61K31/4965 , A61K31/44 , A61K31/47 , C07D413/00 , C07D241/00 , C07D211/00
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）化合物（其中R 1为氢原子，可被取代的烃基，可被取代的非芳香族杂环基，R 2 O 2 >可以被取代的烃基，可以被取代的非芳族杂环基，或者R 1和R 2可以彼此结合形成A至形成可以被取代的杂环基; A是N或N + - - - - - - - （R 5） SUP>为烃基; Y为 - 抗衡阴离子）; R 3为可被取代的环状烃基或可被取代的杂环基; n 为0或1; R 4为氢原子，可被取代的烃基，可被取代的杂环基，可被取代的烷氧基，可被取代的芳氧基，或可以被取代的氨基，E是可以是二价脂族烃基被除氧基以外的基团取代; G 1是一个键，CO或SO 2; G 2是CO，SO 2，NHCO，CONH或OCO; J为次甲基或氮原子; 并且Q和R中的每一个是可被取代的键或二价C 1-3烷基脂族烃; 条件是当G 2 O是OCO时J为次甲基，当另一个为键并且Q和R各自不被氧代基取代时，Q和R中的一个不为键，当G 1是一个键时）或其盐具有强的CCR5拮抗活性，并且可以有利地用于治疗或预防人类各种HIV感染性疾病（如艾滋病）。

8. 发明授权

US06174877B1 Carbapenem compound, their production and use 失效
标题翻译：碳青霉烯化合物，其生产和使用
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。

9. 发明申请

US20140228405A1 CYCLOPROPANEAMINE COMPOUND 有权
标题翻译：环丙烷胺化合物
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。

10. 发明授权

US06562978B1 Cyclic amine compounds as CCR5 antagonists 有权
标题翻译：环胺化合物作为CCR5拮抗剂
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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