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1. 发明授权

US06559166B1 Phenylsulphonyl derivatives as 5-HT receptor ligands 失效
标题翻译：苯磺酰基衍生物作为5-HT受体配体
公开(公告)号：US06559166B1
公开(公告)日：2003-05-06
申请号：US09889702
申请日：2001-09-27
申请人： Peter Blurton , Frank Burkamp , Susan Koon-Fung Cheng , Stephen Robert Fletcher , Angus Murray MacLeod , Daniel Spinks , Monique Bodil Van Niel
发明人： Peter Blurton , Frank Burkamp , Susan Koon-Fung Cheng , Stephen Robert Fletcher , Angus Murray MacLeod , Daniel Spinks , Monique Bodil Van Niel
IPC分类号： A61K31445
CPC分类号： C07D231/12 , C07D211/54 , C07D233/56 , C07D249/08 , C07D401/10
摘要： A class of phenylsulphonyl derivatives wherein the sulphonyl moiety is also attached to an N-arylalkyl-substituted azetidine, pyrrolidine or piperidine ring are selective antagonists of the human 5-HT2A receptor and are therefore useful as pharmaceutical agents, especially in the treatment and/or prevention of adverse conditions of the central nervous system, including schizophrenia and depression.
摘要翻译：一类苯磺酰基衍生物，其中磺酰基部分也连接到N-芳烷基取代的氮杂环丁烷，吡咯烷或哌啶环是人5-HT 2A受体的选择性拮抗剂，因此可用作药剂，特别是在治疗和/或预防中枢神经系统不良状况，包括精神分裂症和抑郁症。

2. 发明授权

US06777430B2 Phenylsulphonyl derivatives as 5-HT receptor ligands 失效
标题翻译：苯磺酰基衍生物作为5-HT受体配体
公开(公告)号：US06777430B2
公开(公告)日：2004-08-17
申请号：US10404188
申请日：2003-04-01
申请人： Peter Blurton , Frank Burkamp , Susan Koon-Fung Cheng , Stephen Robert Fletcher , Angus Murray MacLeod , Daniel Spinks , Monique Bodil Van Niel
发明人： Peter Blurton , Frank Burkamp , Susan Koon-Fung Cheng , Stephen Robert Fletcher , Angus Murray MacLeod , Daniel Spinks , Monique Bodil Van Niel
IPC分类号： A61K314427
CPC分类号： C07D231/12 , C07D211/54 , C07D233/56 , C07D249/08 , C07D401/10
摘要： A class of phenylsulphonyl derivatives wherein the sulphonyl moiety is also attached to an N-arylalkyl-substituted azetidine, pyrrolidine or piperidine ring are selective antagonists of the human 5-HT2A receptor and are therefore useful as pharmaceutical agents, especially in the treatment and/or prevention of adverse conditions of the central nervous system, including schizophrenia and depression.
摘要翻译：一类苯磺酰基衍生物，其中磺酰基部分也连接到N-芳烷基取代的氮杂环丁烷，吡咯烷或哌啶环是人5-HT 2A受体的选择性拮抗剂，因此可用作药剂，特别是在治疗和/或预防中枢神经系统不良状况，包括精神分裂症和抑郁症。

3. 发明授权

US07381725B2 Pyridazine derivatives as ligands for GABA receptors 失效
标题翻译：哒嗪衍生物作为GABA受体的配体
公开(公告)号：US07381725B2
公开(公告)日：2008-06-03
申请号：US10524006
申请日：2003-08-04
申请人： Stephen Robert Fletcher , Angus Murray MacLeod , Monique Bodil Van Niel , Kevin Wilson
发明人： Stephen Robert Fletcher , Angus Murray MacLeod , Monique Bodil Van Niel , Kevin Wilson
IPC分类号： A61K31/501 , C07D401/04 , C07D403/04 , C07D405/04 , C07D409/04 , C07D237/14 , C07D237/20 , A61P25/28
CPC分类号： C07D401/04 , C07D401/14 , C07D403/04 , C07D409/04 , C07D471/04
摘要： A class of pyridazine derivatives, substituted in the 4-position by an optionally substituted heteroaromatic ring, being selective ligands for GABAA receptors, in particular having high 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：一类由任选取代的杂芳环在4-位取代的哒嗪衍生物是GABA A受体的选择性配体，特别是对α2和/或α3和/或其α5亚基具有高亲和力，因此有益于治疗和/或预防中枢神经系统的不良状况，包括焦虑，抽搐和认知障碍。

4. 发明授权

US5998440A Azetidine, pyrrolidine and piperidine derivatives 失效
标题翻译：氮杂环丁烷，吡咯烷和哌啶衍生物
公开(公告)号：US5998440A
公开(公告)日：1999-12-07
申请号：US68620
申请日：1998-05-08
申请人： Jose Luis Castro Pineiro , Angus Murray MacLeod , Monique Bodil Van Niel
发明人： Jose Luis Castro Pineiro , Angus Murray MacLeod , Monique Bodil Van Niel
IPC分类号： C07D521/00 , A61K31/445 , C07D401/06
CPC分类号： C07D231/12 , C07D233/56 , C07D249/08
摘要： A class of substituted azetidine, pyrrolidine and piperidine derivatives, linked by a fluoro-substituted alkylene chain to a fused bicyclic heteroaromatic moiety such as indolyl, are selective agonists of 5-HT.sub.1 -like receptors, being potent agonists of the human 5-HT.sub.1D.alpha. receptor subtype while 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, while eliciting fewer side-effects, notably adverse cardiovascular events, than those associated with non-subtype-selective 5-HT.sub.1D receptor agonists.
摘要翻译： PCT No.PCT / GB96 / 02764 Sec。 371日期1998年5月8日 102（e）日期1998年5月8日PCT 1996年11月13日PCT PCT。第WO97 / 18201号公报日期1997年5月22日一类通过氟取代的亚烷基链连接到稠合双环杂芳族部分如吲哚基的氮杂环丁烷，吡咯烷和哌啶衍生物是5-HT1样受体的选择性激动剂，是人的有效激动剂 5-HT1Dα受体亚型，同时相对于5-HT1Dβ亚型对5-HT1Dα受体亚型具有至少10倍的选择性亲和力; 因此，它们可用于治疗和/或预防临床症状，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，同时引起更少的副作用，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。

5. 发明申请

US20090170824A1 Diarylsulfones as 5-HT2A Antagonists 审中-公开
标题翻译：二芳基砜为5-HT2A拮抗剂
公开(公告)号：US20090170824A1
公开(公告)日：2009-07-02
申请号：US12316388
申请日：2008-12-12
申请人： Jose Luis Castro Pineiro , Laura Catherine Cooper , Myra Gilligan , Alexander Charles Humphries , Peter Alen Hunt , Tamara Ladduwahetty , Angus Murray MacLeod , Kevin John Merchant , Monique Bodil Van Niel , Kevin Wilson
发明人： Jose Luis Castro Pineiro , Laura Catherine Cooper , Myra Gilligan , Alexander Charles Humphries , Peter Alen Hunt , Tamara Ladduwahetty , Angus Murray MacLeod , Kevin John Merchant , Monique Bodil Van Niel , Kevin Wilson
IPC分类号： A61K31/397 , A61K31/47 , A61K31/335 , A61K31/10 , A61K31/535 , A61K31/497
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.
摘要翻译：式I化合物是人5-HT 2A受体的有效和选择性拮抗剂，因此可用于治疗CNS的多种不利条件。

6. 发明授权

US07217740B2 Diarylsulfones as 5-HT2A antagonists 有权
标题翻译：二芳基砜为5-HT2A拮抗剂
公开(公告)号：US07217740B2
公开(公告)日：2007-05-15
申请号：US11212789
申请日：2005-08-26
申请人： Jose Luis Castro Pineiro , Laura Catherine Cooper , Myra Gilligan , Alexander Charles Humphries , Peter Alan Hunt , Tamara Ladduwahetty , Angus Murray MacLeod , Kevin John Merchant , Monique Bodil Van Niel , Kevin Wilson
发明人： Jose Luis Castro Pineiro , Laura Catherine Cooper , Myra Gilligan , Alexander Charles Humphries , Peter Alan Hunt , Tamara Ladduwahetty , Angus Murray MacLeod , Kevin John Merchant , Monique Bodil Van Niel , Kevin Wilson
IPC分类号： A61K31/10 , C07C317/44
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.
摘要翻译：式I的化合物是人5-HT 2A 2A受体的有效和选择性拮抗剂，因此可用于治疗CNS的各种不利条件。

7. 发明授权

US5977116A Piperazine, piperidine and tetrahydropyridine derivatives 失效
标题翻译：哌嗪，哌啶和四氢吡啶衍生物
公开(公告)号：US5977116A
公开(公告)日：1999-11-02
申请号：US68680
申请日：1998-05-12
申请人： Jose Luis Castro Pineiro , Angus Murray MacLeod , Michael Rowley , Monique Bodil Van Niel
发明人： Jose Luis Castro Pineiro , Angus Murray MacLeod , Michael Rowley , Monique Bodil Van Niel
IPC分类号： C07D521/00 , A01N43/60 , C07D401/00 , C07D403/00 , C07D413/00
CPC分类号： C07D231/12 , C07D233/56 , C07D249/08
摘要： A class of N-substituted piperazine, piperidine and tetrahydropyridine derivatives, linked by a fluoro-substituted alkylene chain to a fused bicyclic heteroaromatic moiety such as indolyl, and further substituted at the 4-position by an optionally substituted alkenyl, alkynyl, aryl-alkyl or heteroaryl-alkyl moiety, 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 recptor agonists.
摘要翻译： PCT No.PCT / GB96 / 02762 Sec。 371日期：1998年5月12日 102（e）日期1998年5月12日PCT提交1996年11月13日PCT公布。公开号WO97 / 18203 日期1997年5月22日一类N-取代的哌嗪，哌啶和四氢吡啶衍生物通过氟取代的亚烷基链连接到稠合双环杂芳族部分如吲哚基，并且在4-位被进一步被任选取代的烯基，炔基，芳基 - 烷基或杂芳基 - 烷基部分是5-HT1样受体的选择性激动剂，是人类5-HT1Dα受体亚型的有效激动剂，同时对5-HT1Dα受体具有至少10倍的选择性亲和力亚型相对于5-HT1D beta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。

8. 发明授权

US07468393B2 Diarylsulfones as 5-HT2A antagonists 有权
标题翻译：二芳基砜为5-HT2A拮抗剂
公开(公告)号：US07468393B2
公开(公告)日：2008-12-23
申请号：US11796389
申请日：2007-04-27
申请人： Jose Luis Castro Pineiro , Laura Catherine Cooper , Myra Gilligan , Alexander Charles Humphries , Peter Alan Hunt , Tamara Ladduwahetty , Angus Murray MacLeod , Kevin John Merchant , Monique Bodil Van Niel , Kevin Wilson
发明人： Jose Luis Castro Pineiro , Laura Catherine Cooper , Myra Gilligan , Alexander Charles Humphries , Peter Alan Hunt , Tamara Ladduwahetty , Angus Murray MacLeod , Kevin John Merchant , Monique Bodil Van Niel , Kevin Wilson
IPC分类号： A61K31/10 , C07C317/24 , C07C317/32
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.
摘要翻译：式I化合物是人5-HT 2A受体的有效和选择性拮抗剂，因此可用于治疗CNS的多种不利条件。

9. 发明申请

US20150057273A1 KINASE INHIBITORS 有权
标题翻译：激酶抑制剂
公开(公告)号：US20150057273A1
公开(公告)日：2015-02-26
申请号：US14363556
申请日：2011-12-09
申请人： Harry Finch , Monique Bodil Van Niel , Chi-Kit Woo
发明人： Harry Finch , Monique Bodil Van Niel , Chi-Kit Woo
IPC分类号： C07D471/04 , A61K9/00 , C07D401/12
CPC分类号： C07D471/04 , A61K9/007 , C07D401/12 , C07D403/12
摘要： Disclosed are compounds having [1,2,4]triazolo[4,3-a]pyridine groups and pharmaceutically acceptable salts thereof. The compounds are p38 MAPK inhibitors, useful as anti-inflammatory agents in the treatment of, inter alia, diseases of the respiratory tract.
摘要翻译：公开了具有[1,2,4]三唑并[4,3-a]吡啶基团的化合物及其药学上可接受的盐。这些化合物是p38MAPK抑制剂，其用作治疗特别是呼吸道疾病的抗炎药。

10. 发明授权

US08557797B2 Triazolopyridine derivatives and their therapeutic use 失效
标题翻译：三唑并吡啶衍生物及其治疗用途
公开(公告)号：US08557797B2
公开(公告)日：2013-10-15
申请号：US13201716
申请日：2010-02-16
申请人： Harry Finch , John Montana , Monique Bodil Van Niel , Chi-Kit Woo , Jamie Knight , Bohdan Waszkowycz
发明人： Harry Finch , John Montana , Monique Bodil Van Niel , Chi-Kit Woo , Jamie Knight , Bohdan Waszkowycz
IPC分类号： A61K31/535 , A01N43/54 , C07D413/04 , C07D239/02
CPC分类号： C07D471/04
摘要： Compounds of formula (I) are inhibitors of p38 MAP kinase, useful as anti-inflammatory agents in the treatment of inter alia, diseases of the respiratory tract wherein; R1 is C1-C6 alkyl, C3-C6 cycloalkyl, phenyl which is optionally substituted, 5- or 6 membered monocyclic heteroaryl which is optionally substituted, or a radical of formula (II) wherein n is 1 or 2, and R3 and R4 are independently H or C1-C6 alkyl, or R3 and R4 taken together with the nitrogen to which they are attached form a 6-membered heterocyclic ring optionally containing a further heteroatom selected from N and O; Y is —O— or —S(O)p— wherein p is 0, 1 or 2; A is an optionally substituted divalent arylene radical, or a mono- or bicyclic heteroarylene radical, or a C3-C6 divalent cycloalkylene radical having 5 or 6 ring atoms, or a piperidinylene radical wherein the ring nitrogen is linked to R2NHC(═O)W—; W is a bond, —NH— or —C(RA)(RB), wherein RA and RB are independently H, methyl, ethyl, amino, hydroxyl or halo; and R2 is a radical as defined in the claims.
摘要翻译：式（I）化合物是p38MAP激酶的抑制剂，其可用作治疗特别是呼吸道疾病的抗炎剂，其中： R 1是C 1 -C 6烷基，C 3 -C 6环烷基，任选取代的苯基，任选被取代的5-或6-元单环杂芳基，或其中n是1或2的式（II）基团，R 3和R 4是独立地是H或C 1 -C 6烷基，或者R 3和R 4与它们所连接的氮一起形成任选含有另外选自N和O的杂原子的6元杂环; Y是-O-或-S（O）p - ，其中p是0,1或2; A是任选取代的二价亚芳基或单环或双环亚杂芳基或具有5或6个环原子的C 3 -C 6二价亚环烷基或哌啶子基，其中环氮连接至R 2 NHC（= O）W - ; W是键，-NH-或-C（RA）（RB），其中RA和RB独立地是H，甲基，乙基，氨基，羟基或卤素; 并且R 2是如权利要求中所定义的基团。

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