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1. 发明授权

US07893058B2 Imidazolopyrazine compounds useful for the treatment of degenerative and inflammatory diseases 有权
标题翻译：咪唑并吡嗪类化合物可用于治疗退行性和炎性疾病
公开(公告)号：US07893058B2
公开(公告)日：2011-02-22
申请号：US11803015
申请日：2007-05-11
申请人： Martin James Inglis Andrews , Paul Edwards , Philip Huxley , Wolfgang Schmidt , Veronique Birault , Mark Stuart Chambers , Clifford John Harris , Angus MacLeod , Kim Louise Hirst , Juha Andrew Clase , Gregory Bar
发明人： Martin James Inglis Andrews , Paul Edwards , Philip Huxley , Wolfgang Schmidt , Veronique Birault , Mark Stuart Chambers , Clifford John Harris , Angus MacLeod , Kim Louise Hirst , Juha Andrew Clase , Gregory Bar
IPC分类号： C07D487/04 , A61K31/4985
CPC分类号： C07D487/04
摘要： Novel imidazo[1,2-a]pyrazine compounds are disclosed that have a formula represented by the following: The compounds may be prepared as pharmaceutical compositions, and may be used for the prevention and treatment of a variety of conditions in mammals including humans, including by way of non-limiting example, arthritis, inflammation, and others.
摘要翻译：公开了具有下列表示的式的新型咪唑并[1,2-a]吡嗪化合物：该化合物可以制备为药物组合物，并且可用于预防和治疗包括人在内的哺乳动物中的多种病症，包括作为非限制性实例的关节炎，炎症等。

2. 发明授权

US07915256B2 Triazolopyrazine compounds useful for the treatment of degenerative and inflammatory diseases 失效
标题翻译：可用于治疗退行性和炎性疾病的三唑并吡嗪化合物
公开(公告)号：US07915256B2
公开(公告)日：2011-03-29
申请号：US12399979
申请日：2009-03-08
申请人： Martin James Inglis Andrews , Paul Edwards , Mark Stuart Chambers , Wolfgang Schmidt , Juha Andrew Clase , Gregory Bar , Kim Louise Hirst , Angus MacLeod
发明人： Martin James Inglis Andrews , Paul Edwards , Mark Stuart Chambers , Wolfgang Schmidt , Juha Andrew Clase , Gregory Bar , Kim Louise Hirst , Angus MacLeod
IPC分类号： C07D403/12 , A61K31/506
CPC分类号： C07D487/04
摘要： Novel [1.2.4]triazolo[1,5-a]pyrazine compounds are disclosed that have a formula represented by the following: The compounds may be prepared as pharmaceutical compositions, and may be used for the prevention and treatment of a variety of conditions in mammals including humans, including by way of non-limiting example, pain, inflammation, and others.
摘要翻译：公开了具有下列化学式的新型[1.2.4]三唑并[1,5-a]吡嗪化合物：该化合物可以制备成药物组合物，并可用于预防和治疗各种病症在包括人的哺乳动物中，包括作为非限制性实例的疼痛，炎症等。

3. 发明授权

US07501411B2 Triazolopyrazine compounds useful for the treatment of degenerative and inflammatory diseases 失效
标题翻译：可用于治疗退行性和炎性疾病的三唑并吡嗪化合物
公开(公告)号：US07501411B2
公开(公告)日：2009-03-10
申请号：US11809294
申请日：2007-05-30
申请人： Martin James Inglis Andrews , Paul Edwards , Mark Stuart Chambers , Wolfgang Schmidt , Juha Andrew Clase , Gregory Bar , Kim Louise Hirst , Angus MacLeod
发明人： Martin James Inglis Andrews , Paul Edwards , Mark Stuart Chambers , Wolfgang Schmidt , Juha Andrew Clase , Gregory Bar , Kim Louise Hirst , Angus MacLeod
IPC分类号： C07D487/04 , A61K31/4985
CPC分类号： C07D487/04
摘要： Novel [1.2.4]triazolo[1,5-a]pyrazine compounds are disclosed that have a formula represented by the following: The compounds may be prepared as pharmaceutical compositions, and may be used for the prevention and treatment of a variety of conditions in mammals including humans, including by way of non-limiting example, pain, inflammation, and others.
摘要翻译：公开了具有下列化学式的新型[1.2.4]三唑并[1,5-a]吡嗪化合物：该化合物可以制备成药物组合物，并可用于预防和治疗各种病症在包括人的哺乳动物中，包括作为非限制性实例的疼痛，炎症等。

4. 发明申请

US20100298300A1 TRIAZOLOPYRAZINE COMPOUNDS USEFUL FOR THE TREATMENT OF DEGENERATIVE & INFLAMMATORY DISEASES 失效
标题翻译：用于治疗变应性和炎症性疾病的三唑吡嗪化合物
公开(公告)号：US20100298300A1
公开(公告)日：2010-11-25
申请号：US12399979
申请日：2009-03-08
申请人： Martin James Inglis Andrews , Paul Edwards , Mark Stuart Chambers , Wolfgang Schmidt , Juha Andrew Clase , Gregory Bar , Kim Louise Hirst , Angus MacLeod
发明人： Martin James Inglis Andrews , Paul Edwards , Mark Stuart Chambers , Wolfgang Schmidt , Juha Andrew Clase , Gregory Bar , Kim Louise Hirst , Angus MacLeod
IPC分类号： A61K31/551 , A61K31/5377 , A61K31/519 , C07D487/04 , C07D243/08 , A61P29/00 , A61P19/02 , A61P9/10 , A61P9/00
CPC分类号： C07D487/04
摘要： Novel [1.2.4]triazolo[1,5-a]pyrazine compounds are disclosed that have a formula represented by the following: The compounds may be prepared as pharmaceutical compositions, and may be used for the prevention and treatment of a variety of conditions in mammals including humans, including by way of non-limiting example, pain, inflammation, and others.
摘要翻译：公开了具有下列化学式的新型[1.2.4]三唑并[1,5-a]吡嗪化合物：该化合物可以制备成药物组合物，并可用于预防和治疗各种病症在包括人的哺乳动物中，包括作为非限制性实例的疼痛，炎症等。

5. 发明授权

US08178530B2 Imidazolopyrazine compounds useful for the treatment of degenerative and inflammatory diseases 有权
公开(公告)号：US08178530B2
公开(公告)日：2012-05-15
申请号：US12970632
申请日：2010-12-16
申请人： Martin James Inglis Andrews , Paul Edwards , Reginald Christophe Xavier Brys , Philip Huxley , Wolfgang Schmidt , Veronique Birault , Mark Stuart Chambers , Clifford John Harris , Angus MacLeod , Kim Louise Hirst , Juha Andrew Clase , Gregory Bar
发明人： Martin James Inglis Andrews , Paul Edwards , Reginald Christophe Xavier Brys , Philip Huxley , Wolfgang Schmidt , Veronique Birault , Mark Stuart Chambers , Clifford John Harris , Angus MacLeod , Kim Louise Hirst , Juha Andrew Clase , Gregory Bar
IPC分类号： C07D487/04 , A61K31/4985
CPC分类号： C07D487/04
摘要： Novel imidazo[1,2-a]pyrazine compounds are disclosed that have a formula represented by the following: The compounds may be prepared as pharmaceutical compositions, and may be used for the prevention and treatment of a variety of conditions in mammals including humans, including by way of non-limiting example, arthritis, inflammation, and others.

6. 发明申请

US20080090818A1 Triazolopyrazine compounds useful for the treatment of degenerative & inflammatory diseases 失效
标题翻译：用于治疗退行性和炎性疾病的三唑并吡嗪化合物
公开(公告)号：US20080090818A1
公开(公告)日：2008-04-17
申请号：US11809294
申请日：2007-05-30
申请人： Martin James Andrews , Paul Edwards , Mark Chambers , Wolfgang Schmidt , Juha Clase , Gregory Bar , Kim Hirst , Angus MacLeod
发明人： Martin James Andrews , Paul Edwards , Mark Chambers , Wolfgang Schmidt , Juha Clase , Gregory Bar , Kim Hirst , Angus MacLeod
IPC分类号： A61K31/5355 , A61K31/5025 , A61P19/02 , C07D403/02 , C07D413/14 , C07D471/04
CPC分类号： C07D487/04
摘要： Novel [1.2.4]triazolo[1,5-a]pyrazine compounds are disclosed that have a formula represented by the following: The compounds may be prepared as pharmaceutical compositions, and may be used for the prevention and treatment of a variety of conditions in mammals including humans, including by way of non-limiting example, pain, inflammation, and others.
摘要翻译：公开了具有下列化学式的新型[1.2.4]三唑并[1,5-a]吡嗪化合物：该化合物可以制备成药物组合物，并可用于预防和治疗各种病症在包括人的哺乳动物中，包括作为非限制性实例的疼痛，炎症等。

7. 发明申请

US20070203205A1 Diarylsulfones as 5-HT2A antagonists 有权
公开(公告)号：US20070203205A1
公开(公告)日：2007-08-30
申请号：US11796389
申请日：2007-04-27
申请人： Jose Castro Pineiro , Laura Cooper , Myra Gilligan , Alexander Humphries , Peter Hunt , Tamara Ladduwahetty , Angus MacLeod , Kevin Merchant , Monique Van Niel , Kevin Wilson
发明人： Jose Castro Pineiro , Laura Cooper , Myra Gilligan , Alexander Humphries , Peter Hunt , Tamara Ladduwahetty , Angus MacLeod , Kevin Merchant , Monique Van Niel , Kevin Wilson
IPC分类号： A61K31/4245 , A61K31/4164 , A61K31/235 , A61K31/10
CPC分类号： C07C317/28 , C07C317/14 , C07C317/22 , C07C317/24 , C07C317/32 , C07C317/36 , C07C317/42 , C07C317/44 , C07D205/04 , C07D207/10 , C07D211/38 , C07D211/72 , C07D213/34 , C07D213/71 , C07D217/24 , C07D231/12 , C07D233/64 , C07D241/08 , C07D249/08 , C07D261/08 , C07D271/10 , C07D277/26 , C07D295/096 , C07D317/62 , C07D319/18
摘要： Compounds of formula I: are potent and selective antagonists of the human 5-HT2A receptor, and hence useful in treatment of a variety of adverse conditions of the CNS.

8. 发明申请

US20060089348A1 Substituted quinoline-4-carboxylic hydrazides as nk-2/nk-3 receptor ligands 失效
标题翻译：取代的喹啉-4-羧酸酰肼作为nk-2 / nk-3受体配体
公开(公告)号：US20060089348A1
公开(公告)日：2006-04-27
申请号：US10544440
申请日：2004-02-03
申请人： Mark Chambers , Philip Jones , Angus MacLeod
发明人： Mark Chambers , Philip Jones , Angus MacLeod
IPC分类号： A61K31/55 , A61K31/47 , A61K31/496 , C07D215/38 , C07D403/02
CPC分类号： C07D215/52
摘要： The present invention discloses a compound of formula (I): wherein: R1 is an aryl or heteroaryl ring; R2 is hydroxy, C1-6 alkoxy, C1-6 alkyl, amino, NR′R″ or C1-6 alkyl-NR′R″ where R′ and R″ are independently chosen from hydrogen and C1-4 alkyl and where R′ and R″, together with the nitrogen atom to which they are attached, form a saturated nitrogen-containing 3-7 membered heterocycle optionally containing a further nitrogen atom and optionally substituted by NR′R″ as defined above or R2 is C1-6 alkoxy substituted by NR′R″ as defined above; R3 is hydrogen or C1-6 alkyl; R4 is hydrogen, C1-8 alkyl, C2-8 alkenyl, C2-8 alkynyl, C3-8 cycloalkyl, aryl or aryl C1-6 alkyl; R5 is hydrogen, C1-8 alkyl, C2-8 alkenyl, C2-8 alkynyl, C3-8 cycloalkyl, aryl, aryl C1-6 alkyl or C1-6 alkoxycarbonyl; or R4 and R5, together with the nitrogen atom to which they are attached, form a C3-C10 mono- or bicyclic saturated ring; X and Y are independently chosen from hydrogen, hydroxy, nitro, amino, cyano, CF3, halogen and C1-4 alkyl; or a pharmaceutically acceptable salt thereof; as NK-2/NK-3 ligands for treating schizophrenia, COPD, asthma or irritable bowel syndrome.
摘要翻译：本发明公开了式（I）的化合物：其中：R 1是芳基或杂芳基环; R 2是羟基，C 1-6烷氧基，C 1-6烷基，氨基，NR'R“或C” 1-6烷基-NR'R“，其中R'和R”独立地选自氢和C 1-4烷基，并且其中R'和R“与它们所连接的氮原子形成饱和的含氮3-7元杂环，其任选地含有另外的氮原子，并且任选地被如上所定义的NR'R“或R 2取代为C 被如上所定义的NR'R“取代的1-6位的烷氧基; R 3是氢或C 1-6烷基; R 4是氢，C 1-8 - 烷基，C 2-8 - 烯基，C 2-8 - 炔基 C 3-8环烷基，芳基或芳基C 1-6烷基; R 5是氢，C 1-8 - 烷基，C 2-8 - 烯基，C 2-8 - 炔基 C 3 -C 8环烷基，芳基，芳基C 1-6烷基或C 1-6烷氧基羰基; 或R 4和R 5与它们所连接的氮原子一起形成C 3 -C 10烷基， / SUB单环或双环饱和环; X和Y独立地选自氢，羟基，硝基，氨基，氰基，CF 3，卤素和C 1-4烷基; 或其药学上可接受的盐; 作为用于治疗精神分裂症，COPD，哮喘或肠易激综合征的NK-2 / NK-3配体。

9. 发明申请

US20050101586A1 Novel 5-HT2A receptor ligands 失效
标题翻译：新型5-HT2A受体配体
公开(公告)号：US20050101586A1
公开(公告)日：2005-05-12
申请号：US10984249
申请日：2004-11-09
申请人： Mark Chambers , Neil Curtis , Angus MacLeod , Robert Maxey , Helen Szekeres
发明人： Mark Chambers , Neil Curtis , Angus MacLeod , Robert Maxey , Helen Szekeres
IPC分类号： C07D205/04 , C07D401/06 , C07D401/12 , C07D403/12 , C07D409/06 , C07D413/06 , C07D417/06 , C07D417/14 , C07D495/04 , A61K31/397 , C07D413/02 , C07D417/02 , C07D43/02
CPC分类号： C04B35/632 , C07D205/04 , C07D401/06 , C07D401/12 , C07D403/12 , C07D409/06 , C07D413/06 , C07D417/06 , C07D417/14 , C07D495/04
摘要： Compounds of formula I: are antagonists of the human 5-HT2A receptor, and hence useful in treatment or prevention of a variety of neurological conditions.
摘要翻译：式I化合物是人5-HT 2A 2A受体的拮抗剂，因此可用于治疗或预防各种神经病症。

10. 发明授权

US08362018B2 Substituted imidazo[1,2-a]pyrazine compounds useful for the treatment of viral infections 失效
标题翻译：用于治疗病毒感染的取代的咪唑并[1,2-a]吡嗪化合物
公开(公告)号：US08362018B2
公开(公告)日：2013-01-29
申请号：US12674525
申请日：2008-08-20
申请人： Angus MacLeod , Dale Robert Mitchell , Nicholas John Palmer , Michael Daniel Goldsmith , Clifford John Harris , Christophe Claude Parsy
发明人： Angus MacLeod , Dale Robert Mitchell , Nicholas John Palmer , Michael Daniel Goldsmith , Clifford John Harris , Christophe Claude Parsy
IPC分类号： A61K31/495
CPC分类号： C07D487/04
摘要： Novel imidazopyrazine compounds are disclosed that have a formula represented by the following: The compounds may be prepared as pharmaceutical compositions, and may be used for the prevention and treatment of a viral infection, in particular a HCV, HRV, Sb and/or CVB in a patient in need thereof.
摘要翻译：公开了具有下列表示的式的新型咪唑并吡嗪化合物：该化合物可以制备成药物组合物，并可用于预防和治疗病毒感染，特别是HCV，HRV，Sb和/或CVB中的HCV 有需要的患者。

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