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11. 发明申请

US20100010053A1 COMPOUNDS 审中-公开
标题翻译：化合物
公开(公告)号：US20100010053A1
公开(公告)日：2010-01-14
申请号：US12486853
申请日：2009-06-18
申请人： Jose Luis Castro Pineiro , Xichen Lin , Qian Liu , Kevin Meng , Feng Ren , David R. Vesey , Baowei Zhao
发明人： Jose Luis Castro Pineiro , Xichen Lin , Qian Liu , Kevin Meng , Feng Ren , David R. Vesey , Baowei Zhao
IPC分类号： A61K31/4245 , C07D271/06 , A61P37/06 , A61P29/00 , A61P35/00 , A61P1/00
CPC分类号： C07D413/04 , C07D413/14
摘要： The present invention relates to novel oxadiazole derivatives having pharmacological activity, processes for their preparation, pharmaceutical compositions containing them and their use in the treatment of various disorders.
摘要翻译：本发明涉及具有药理活性的新型恶二唑衍生物，其制备方法，含有它们的药物组合物及其在治疗各种病症中的用途。

12. 发明授权

US07626056B2 Cyclohexanesulfonyl derivatives as GlyT1 inhibitors to treat schizophrenia 有权
标题翻译：环己磺酰基衍生物作为治疗精神分裂症的GlyT1抑制剂
公开(公告)号：US07626056B2
公开(公告)日：2009-12-01
申请号：US11446735
申请日：2006-06-05
申请人： Wesley Peter Blackaby , Jose Luis Castro Pineiro , Richard Thomas Lewis , Elizabeth Mary Naylor , Leslie Joseph Street
发明人： Wesley Peter Blackaby , Jose Luis Castro Pineiro , Richard Thomas Lewis , Elizabeth Mary Naylor , Leslie Joseph Street
IPC分类号： C07C233/65 , A61K31/16
CPC分类号： C07D213/82 , C07C233/70 , C07C233/76 , C07C317/30 , C07C2601/02 , C07C2601/14 , C07D231/12 , C07D231/18 , C07D239/28 , C07D249/04 , C07D285/125 , C07D295/108 , C07D295/135 , C07D307/68 , C07D333/38 , C07D471/04 , C07D495/04
摘要： The present invention provides compounds of formula I: wherein R1 is an alkyl, phenyl, heterocyclyl, cycloalkyl, alkoxy, ester, amino or amide group; R2 is a phenyl, heterocyclyl, alkyl, cycloalkyl or cycloalkylalkyl group; R3 is an alkyl, cycloalkyl, cycloalkylalkyl, amino or heterocyclyl group; R4 and R5 are hydrogen or alkyl or form a cycloalkyl ring; A is O or N; and m is zero or one; as inhibitors of GlyT1 and thus as useful for treating or preventing diseases such as schizophrenia; with the provision of pharmaceutical compositions, first and second medical uses and methods of treatment.
摘要翻译：本发明提供式I化合物：其中R 1是烷基，苯基，杂环基，环烷基，烷氧基，酯，氨基或酰胺基; R2是苯基，杂环基，烷基，环烷基或环烷基烷基; R3是烷基，环烷基，环烷基烷基，氨基或杂环基; R4和R5是氢或烷基或形成环烷基环; A是O或N; m为零或一; 作为GlyT1的抑制剂，因此可用于治疗或预防精神分裂症等疾病; 提供药物组合物，第一和第二医疗用途和治疗方法。

13. 发明授权

US07049296B2 Gamma-secretase inhibitors 失效
标题翻译： γ-分泌酶抑制剂
公开(公告)号：US07049296B2
公开(公告)日：2006-05-23
申请号：US10204962
申请日：2001-02-28
申请人： Jose Luis Castro Pineiro , Adrian Leonard Smith , Graeme Irvine Stevenson
发明人： Jose Luis Castro Pineiro , Adrian Leonard Smith , Graeme Irvine Stevenson
IPC分类号： A61K38/05 , C07C271/00 , C07K5/06
CPC分类号： C07K5/06034 , A61K38/00 , C07K5/06026 , C07K5/06078
摘要： Urea derivatives of formula I are disclosed: The compounds are inhibitors of γ-secretase, and hence useful in the treatment or prevention of Alzheimer's Disease
摘要翻译：公开了式I的脲衍生物：该化合物是γ-分泌酶的抑制剂，因此可用于治疗或预防阿尔茨海默病

14. 发明授权

US07030128B2 Imidazo-pyrimidine derivatives as ligands for GABA receptors 失效
标题翻译：咪唑并嘧啶衍生物作为GABA受体的配体
公开(公告)号：US07030128B2
公开(公告)日：2006-04-18
申请号：US10472680
申请日：2002-03-19
申请人： Wesley Peter Blackaby , Jose Luis Castro Pineiro , Mark Stuart Chambers , Simon Charles Goodacre , David James Hallett , Philip Jones , Richard Thomas Lewis , Angus Murray MacLeod , Robert James Maxey , Kevin William Moore , Leslie Joseph Street
发明人： Wesley Peter Blackaby , Jose Luis Castro Pineiro , Mark Stuart Chambers , Simon Charles Goodacre , David James Hallett , Philip Jones , Richard Thomas Lewis , Angus Murray MacLeod , Robert James Maxey , Kevin William Moore , Leslie Joseph Street
IPC分类号： A61K31/519 , C07D487/04 , A61P25/22
CPC分类号： C07D487/04 , A61K31/519
摘要： A class of imidazo[1,2-α]pyrimidine derivatives, substituted at the 3-position by an optionally substituted five-membered or six-membered heteroaromatic ring, are selective ligands for GABAA receptors, in particular having good affinity for the α2 and/or α3 and/or α5 subunit thereof, and 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3-位上被取代的咪唑并[1,2-α]嘧啶衍生物，是GABA A A受体的选择性配体，特别是对α2和/或α3和/或α5亚基具有良好的亲和力，因此有益于治疗和/或预防中枢神经系统的不利条件，包括焦虑，抽搐和认知障碍。

15. 发明授权

US06828322B2 Triazolo-pyridazine derivatives as ligands for GABA receptors 失效
标题翻译：三唑并哒嗪衍生物作为GABA受体的配体
公开(公告)号：US06828322B2
公开(公告)日：2004-12-07
申请号：US10463075
申请日：2003-06-17
申请人： William Robert Carling , Jose Luis Castro Pineiro , Ian James Collins , Alexander Richard Guiblin , Timothy Harrison , Andrew Madin , Kevin William Moore , Michael Geoffrey Russell , Gayle Scott , Leslie Joseph Street
发明人： William Robert Carling , Jose Luis Castro Pineiro , Ian James Collins , Alexander Richard Guiblin , Timothy Harrison , Andrew Madin , Kevin William Moore , Michael Geoffrey Russell , Gayle Scott , Leslie Joseph Street
IPC分类号： A61K315025
CPC分类号： C07D487/04
摘要： A class of substituted 1,2,4-triazolo[4,3-b]pyridazine derivatives, possessing a fluoro-substituted phenyl ring at the 3-position and a heteroaryl-methoxy moiety at the 6-position, are selective ligands for GABAA receptors, in particular having high affinity for the &agr;2 and/or &agr;3 subunit thereof, and are accordingly of benefit in the treatment and/or prevention of disorders of the central nervous system, including anxiety and convulsions.
摘要翻译：在3-位上具有氟取代的苯环和6-位上的杂芳基 - 甲氧基部分的一类取代的1,2,4-三唑并[4,3-b]哒嗪衍生物是GABAA的选择性配体受体，特别是对其α2和/或α3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疾病，包括焦虑和抽搐。

16. 发明授权

US06187805B1 Indole and indoline derivatives as 5-HT6 selective ligands 失效
标题翻译：吲哚和二氢吲哚衍生物作为5-HT6选择性配体
公开(公告)号：US06187805B1
公开(公告)日：2001-02-13
申请号：US09392406
申请日：1999-09-09
申请人： Jose Luis Castro Pineiro , George Mc Allister , Michael Geoffrey Neil Russel
发明人： Jose Luis Castro Pineiro , George Mc Allister , Michael Geoffrey Neil Russel
IPC分类号： A61K31405
CPC分类号： A61K31/404 , A61K31/4045 , C07D209/08 , C07D209/12 , C07D209/14 , C07D209/16 , C07D209/90 , C07D409/12
摘要： Three classes of indole and indoline derivatives are disclosed as ligands selective for the 5-HT6 receptors, and hence of value in the treatment or prevention of CNS disorders, including Alzheimer's disease, Parkinson's disease, schizophrenia, depression and anxiety. A particular class, 1-substituted-4-(&ohgr;-N,N-dialkyl-aminoalkyl)indoles, are claimed as novel compounds.
摘要翻译：公开了三类吲哚和二氢吲哚衍生物作为对5-HT6受体选择性的配体，因此在治疗或预防包括阿尔茨海默病，帕金森病，精神分裂症，抑郁和焦虑的CNS疾病中具有价值。作为新化合物，要求具体的1-取代-4-（ω-N，N-二烷基 - 氨基烷基）吲哚类。

17. 发明授权

US6051572A 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：US6051572A
公开(公告)日：2000-04-18
申请号：US68066
申请日：1998-04-28
申请人： Jose Luis Castro Pineiro
发明人： Jose Luis Castro Pineiro
IPC分类号： C07D521/00 , C07D401/14 , A61K31/445 , C07D403/14
CPC分类号： C07D231/12 , C07D233/56 , C07D249/08
摘要： A class of azetidine, pyrrolidine and piperidine derivatives, substituted by inter alia a phenylmorpholinyl, phenylpiperidinyl or benzimidazolone 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 receptor agonists.
摘要翻译： PCT No.PCT / GB96 / 02625 Sec。 371日期：1998年4月28日 102（e）1998年4月28日PCT PCT 1996年10月28日PCT公布。出版物WO97 / 16445 日期1997年5月9日一类被苯基吗啉基，苯基哌啶基或苯并咪唑酮部分取代的氮杂环丁烷，吡咯烷和哌啶衍生物是5-HT1样受体的选择性激动剂，是人类5-HT1Dα受体亚型的有效激动剂，对5-HT1Dα受体亚型相对于5-HT1Dβ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。

18. 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。

19. 发明申请

US20120190672A1 FUSED AMINODIHYDROTHIAZINE DERIVATIVES 有权
标题翻译：熔融氨基二氢卟吩衍生物
公开(公告)号：US20120190672A1
公开(公告)日：2012-07-26
申请号：US13354716
申请日：2012-01-20
申请人： Adrian Hall , Christopher Neil Farthing , Jose Luis Castro Pineiro
发明人： Adrian Hall , Christopher Neil Farthing , Jose Luis Castro Pineiro
IPC分类号： A61K31/542 , A61P25/28 , A61P3/10 , C07D513/04
CPC分类号： C07D513/04
摘要： The present invention relates to a fused aminodihydrothiazine derivative of formula (I): wherein X is hydrogen or fluorine; A is CH or N; Y is methyl, ethyl, monofluoromethyl, difluoromethyl, trifluoromethyl, difluoroethyl, methoxy, ethoxy, methoxymethyl or —C≡N; and pharmaceutically acceptable salts thereof; which compound has an Aβ production inhibitory effect or a BACE1 inhibitory effect and is useful as a prophylactic or therapeutic agent for a neurodegenerative disease caused by Aβ and typified by Alzheimer-type dementia.
摘要翻译：本发明涉及式（I）的稠合氨基二氢噻嗪衍生物：其中X是氢或氟; A是CH或N; Y是甲基，乙基，一氟甲基，二氟甲基，三氟甲基，二氟乙基，甲氧基，乙氧基，甲氧基甲基或-C≡N; 及其药学上可接受的盐; 该化合物具有A＆bgr; 产生抑制作用或BACE1抑制作用，可用作由A＆Bgr引起的神经变性疾病的预防或治疗剂; 并以阿尔茨海默氏型痴呆为代表。

20. 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。

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