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41. 发明授权

US5919783A Indoline and azaindoline derivatives as 5-HT.sub.1D alpha receptor agonists 失效
标题翻译：二氢吲哚和唑啉衍生物作为5-HT1Dα受体激动剂
公开(公告)号：US5919783A
公开(公告)日：1999-07-06
申请号：US776626
申请日：1997-01-21
申请人： Mark Stuart Chambers , Victor Giulio Matassa , Leslie Joseph Street
发明人： Mark Stuart Chambers , Victor Giulio Matassa , Leslie Joseph Street
IPC分类号： C07D521/00 , A61K31/495 , C07D403/14 , C07D471/04
CPC分类号： C07D231/12 , C07D233/56 , C07D249/08
摘要： Compounds of formula (I), or a salt or prodrug thereof, wherein Z represents an optionally substituted five-membered heteroaromatic ring selected from furan, thiophene, pyrrole, oxazole, thiazole, isoxazole, isothiazole, imidazole, pyrazole, oxadiazole, thiadiazole, triazole, and tetrazole; E represents a chemical bond or a straight or branched alkylene chain containing from 1-4 carbon atoms; Q represents a straight or branched alkylene chain containing from 1-6 carbon atoms; T represents nitrogen or CH; R.sup.1 represents aryl(C.sub.1-6)alkyl or heteroaryl(C.sub.1-6)alkyl, either of which groups may be optionally substituted; and R.sup.2 represents hydrogen or C.sub.1-6 alkyl are selective agonists of 5-HT.sub.1 -like receptors, being potent agonists of the human 5-HT.sub.1D.alpha. receptor subtype whilst possessing at least a 10-fold selective affinity for the 5-HT.sub.1D.alpha. receptor subtype relative to the 5-HT.sub.1D.beta. subtype; they are therefore useful in the treatment and/or prevention of clinical conditions, in particular migraine and associated disorders, for which a subtype-selective agonist of 5-HT.sub.1D receptors is indicated, whilst eliciting fewer side-effects, notably adverse cardiovascular events, than those associated with non-subtype-selective 5-HT.sub.1D receptor agonists. ##STR1##
摘要翻译： PCT No.PCT / GB95 / 01756 Sec。 371日期1997年1月21日 102（e）1997年1月21日PCT PCT 1995年7月24日PCT公布。出版物WO96 / 04269 日期：2002年2月15日式（I）化合物或其盐或前体药物，其中Z表示选自呋喃，噻吩，吡咯，恶唑，噻唑，异恶唑，异噻唑，咪唑，吡唑等的任选取代的五元杂芳族环，恶二唑，噻二唑，三唑和四唑; E表示化学键或含有1-4个碳原子的直链或支链亚烷基链; Q表示含有1-6个碳原子的直链或支链亚烷基链; T表示氮或CH; R1表示芳基（C1-6）烷基或杂芳基（C1-6）烷基，其中任一个可以任选被取代; 并且R 2表示氢或C 1-6烷基是5-HT1样受体的选择性激动剂，其是人5-HT1Dα受体亚型的有效激动剂，同时对5-HT1Dα受体亚型具有至少10倍的选择性亲和力相对于5-HT1Dβ亚型; 因此，它们可用于治疗和/或预防临床状况，特别是偏头痛和相关疾病，其中指出5-HT1D受体的亚型选择性激动剂，同时引起较少的副作用，特别是不利的心血管事件，比与非亚型选择性5-HT1D受体激动剂相关的那些。

42. 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.

43. 发明授权

US08173656B2 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：US08173656B2
公开(公告)日：2012-05-08
申请号：US12970659
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.
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。

44. 发明申请

US20110178067A1 TRIAZOLOPYRAZINE COMPOUNDS USEFUL FOR THE TREATMENT OF DEGENERATIVE AND INFLAMMATORY DISEASES 审中-公开
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：US20110178067A1
公开(公告)日：2011-07-21
申请号：US12987129
申请日：2011-01-09
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 , C07D487/04 , A61K31/4985 , C07D413/14 , A61K31/5377 , A61P29/00 , A61P19/02
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。

45. 发明申请

US20110092497A1 IMIDAZOLOPYRAZINE COMPOUNDS USEFUL FOR THE TREATMENT OF DEGENERATIVE AND INFLAMMATORY DISEASES 有权
公开(公告)号：US20110092497A1
公开(公告)日：2011-04-21
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 , A61K31/5377 , A61K31/4985 , A61P19/02
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.

46. 发明申请

US20090012078A1 Fused pyrazine compounds useful for the treatment of degenerative and inflammatory diseases 有权
标题翻译：用于治疗退行性和炎性疾病的吡唑嗪化合物
公开(公告)号：US20090012078A1
公开(公告)日：2009-01-08
申请号：US12151585
申请日：2008-05-07
申请人： Martin James Inglis Andrews , Mark Stuart Chambers , Wolfgang Schmidt , Giovanni Alessandro Tricarico , Gregory Louis Joseph Bar , Kim Louise Hirst , Olga Raquel Pinto Santos Oliveira Roussel , Juha Andrew Clase
发明人： Martin James Inglis Andrews , Mark Stuart Chambers , Wolfgang Schmidt , Giovanni Alessandro Tricarico , Gregory Louis Joseph Bar , Kim Louise Hirst , Olga Raquel Pinto Santos Oliveira Roussel , Juha Andrew Clase
IPC分类号： A61K31/5377 , C07D413/14 , A61K31/4985 , A61P19/02 , C07D471/04
CPC分类号： C07D487/04
摘要： Novel fused 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, inflammation, rheumatoid arthritis and others.
摘要翻译：公开了具有下列表示的式的新型稠合吡嗪化合物：该化合物可以制备成药物组合物，并且可用于预防和治疗包括人在内的哺乳动物中的各种病症，包括以非限制性方式例如炎症，类风湿关节炎等。

47. 发明授权

US07176203B2 Imidazo-triazine derivatives as ligands for gaba receptors 失效
标题翻译：咪唑并三嗪衍生物作为gaba受体的配体
公开(公告)号：US07176203B2
公开(公告)日：2007-02-13
申请号：US10512608
申请日：2003-05-01
申请人： Mark Stuart Chambers , Simon Charles Goodacre , David James Hallett , Robert James Maxey , Michael Geoffrey Neil Russell , Leslie Joseph Street
发明人： Mark Stuart Chambers , Simon Charles Goodacre , David James Hallett , Robert James Maxey , Michael Geoffrey Neil Russell , Leslie Joseph Street
IPC分类号： C07D487/04 , C07D403/04 , A61K31/53 , A61P25/22
CPC分类号： C07D487/04
摘要： A class of imidazo[1,2b][1,2,4]triazine derivatives, substituted at the 7-position by an optionally substituted five-membered or six-membered heteroaromatic ring, being selective ligands for GABAA receptors, in particular having good affinity for the α2 and/or α3 and/or α5 subunit thereof, are accordingly of benefit in the treatment and/or prevention of adverse conditions of the central nervous system, including anxiety, convulsions and cognitive disorders.
摘要翻译：一类由任选取代的五元或六元杂芳环在7-位取代的咪唑并[1,2b] [1,2,4]三嗪衍生物，是GABA A，特别是具有对α2和/或α3和/或α5亚基具有良好亲和力的受体，因此在治疗和/或预防中枢神经系统的不良状况（包括焦虑，惊厥和认知障碍）方面是有益的。

48. 发明授权

US5719147A Morpholine and thiomorpholine tachykinin receptor antagonists 失效
公开(公告)号：US5719147A
公开(公告)日：1998-02-17
申请号：US525259
申请日：1995-09-08
申请人： Conrad P. Dorn , Paul E. Finke , Jeffrey J. Hale , Malcolm MacCoss , Sander G. Mills , Shrenik K. Shah , Mark Stuart Chambers , Timothy Harrison , Tamara Ladduwahetty , Brian John Williams
发明人： Conrad P. Dorn , Paul E. Finke , Jeffrey J. Hale , Malcolm MacCoss , Sander G. Mills , Shrenik K. Shah , Mark Stuart Chambers , Timothy Harrison , Tamara Ladduwahetty , Brian John Williams
IPC分类号： C07D265/30 , C07D265/32 , C07D279/12 , C07D413/04 , C07D413/06 , C07D413/14 , A61K31/54 , A61K31/535 , C07D417/04
CPC分类号： C07D265/30 , C07D265/32 , C07D279/12 , C07D413/04 , C07D413/06 , C07D413/14 , Y10S514/825
摘要： Substituted heterocycles of the general structural formula: ##STR1## are tachykinin receptor antagonists useful in the treatment of inflammatory diseases, pain or migraine, asthma and emesis, and calcium channel blockers useful in the treatment of cardiovascular conditions such as angina, hypertension or ischemia.

49. 发明授权

US08148369B2 Fused pyrazine compounds useful for the treatment of degenerative and inflammatory diseases 有权
公开(公告)号：US08148369B2
公开(公告)日：2012-04-03
申请号：US12151585
申请日：2008-05-07
申请人： Martin James Inglis Andrews , Mark Stuart Chambers , Wolfgang Schmidt , Giovanni Alessandro Tricarico , Grégory Louis Joseph Bar , Kim Louise Hirst , Olga Raquel Pinto Santos Oliveira Roussel , Juha Andrew Clase
发明人： Martin James Inglis Andrews , Mark Stuart Chambers , Wolfgang Schmidt , Giovanni Alessandro Tricarico , Grégory Louis Joseph Bar , Kim Louise Hirst , Olga Raquel Pinto Santos Oliveira Roussel , Juha Andrew Clase
IPC分类号： A61K31/50 , A61K31/535 , C07D413/14 , C07D471/04
CPC分类号： C07D487/04
摘要： Novel fused 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, inflammation, rheumatoid arthritis and others.

50. 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。

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