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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。

5. 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。

6. 发明授权

US6136824A 1-piperidinyl-propan-2-derivatives and their use as therapeutic agents 失效
标题翻译： 1-哌啶基 - 丙-2-衍生物及其作为治疗剂的用途
公开(公告)号：US6136824A
公开(公告)日：2000-10-24
申请号：US511002
申请日：2000-02-22
申请人： Angus Murray MacLeod , Christopher John Swain , Monique Bodil van Niel
发明人： Angus Murray MacLeod , Christopher John Swain , Monique Bodil van Niel
IPC分类号： A61P25/00 , A61P29/00 , C07D211/22 , C07D405/12 , A01N43/40
CPC分类号： C07D405/12 , C07D211/22
摘要： The present invention relates compounds of the formula (I): ##STR1## wherein R.sup.1 and R.sup.2 each independently represents a phenyl group optionally substituted by a variety of substituents;R.sup.3 represents a variety of substituents;R.sup.4, R.sup.5, R.sup.6, and R.sup.7 each independently represents hydrogen or C.sub.1-6 alkyl;A represents --O-- or --S--;B represents --O--, --S--, --NR.sup.a -- or --CHR.sup.a --; andn is zero, 1, 2, 3, 4 or 5;or a pharmaceutically acceptable salt or a prodrug thereof.The compounds are of particular use in the treatment or prevention of depression, anxiety, pain, inflammation, migaine, emesis or postherpetic neuralgia.
摘要翻译：本发明涉及式（I）的化合物：其中R 1和R 2各自独立地表示任选被各种取代基取代的苯基; R3代表各种取代基; R4，R5，R6和R7各自独立地表示氢或C1-6烷基; A表示-O-或-S-; B表示-O - ， - S - ， - NR a - 或-CHRa-; 并且n为零，1,2,3,4或5; 或其药学上可接受的盐或前药。这些化合物特别用于治疗或预防抑郁，焦虑，疼痛，炎症，迁移物，呕吐或带状疱疹后神经痛。

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。

10. 发明授权

US07482457B2 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：US07482457B2
公开(公告)日：2009-01-27
申请号：US10544440
申请日：2004-02-03
申请人： Mark Stuart Chambers , Philip Jones , Angus Murray MacLeod
发明人： Mark Stuart Chambers , Philip Jones , Angus Murray MacLeod
IPC分类号： C07D215/38
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：R1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，其中R'和R“与它们所连接的氮原子一起形成任选含有另外的氮原子并且任选地被如上所定义的NR'R”取代的饱和含氮3-7元杂环或R2 是由如上定义的NR'R“取代的C 1-6烷氧基; R3是氢或C1-6烷基; R4是氢，C1-8烷基，C2-8烯基，C2-8炔基，C3-8环烷基，芳基或芳基C1-6烷基; R5是氢，C1-8烷基，C2-8烯基，C2-8炔基，C3-8环烷基，芳基，芳基C1-6烷基或C1-6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。

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