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1. 发明授权

US06355638B1 Pyrazolo[1,5-d][1,2,4] triazines for enhancing cognition 有权
标题翻译：吡唑并[1,5-d] [1,2,4]三嗪用于增强认知
公开(公告)号：US06355638B1
公开(公告)日：2002-03-12
申请号：US09717423
申请日：2000-11-21
申请人： Helen Jane Bryant , William Robert Carling , Mark Stuart Chambers , Sarah Christine Hobbs , Philip Jones , Angus Murray MacLeod
发明人： Helen Jane Bryant , William Robert Carling , Mark Stuart Chambers , Sarah Christine Hobbs , Philip Jones , Angus Murray MacLeod
IPC分类号： C07D48714
CPC分类号： C07D487/04
摘要： Compounds according to Formula (I) or a salt thereof are GABA-A Alpha 5 ligands useful for enhancing cognition:
摘要翻译：根据式（I）的化合物或其盐是可用于增强认知的GABA-Aα5配体：

2. 发明授权

US07144887B2 Substituted 1,2,3-triazolo[1,5-a]quinazolines for enhancing cognition 失效
标题翻译：取代的1,2,3-三唑并[1,5-a]喹唑啉用于增强认知
公开(公告)号：US07144887B2
公开(公告)日：2006-12-05
申请号：US10149852
申请日：2000-12-11
申请人： Helen Jane Bryant , Mark Stuart Chambers , Philip Jones , Angus Murray MacLeod , Robert James Maxey
发明人： Helen Jane Bryant , Mark Stuart Chambers , Philip Jones , Angus Murray MacLeod , Robert James Maxey
IPC分类号： A61K471/04 , A61K31/505 , C07D239/00 , C07D471/00 , C07D487/00
CPC分类号： C07D487/04
摘要： The present invention provides a compound of formula (I) in which R1 is generally hydrogen or CF3, R2 is generally hydrogen, W is a cyclic amine, a heterocycle or a group L-Y—X where L-Y is a linking portion and X is generally an aromatic or non-aromatic heterocycle, alkyl or alkylcarbonyl and Z is generally a heterocycle such as 5-methylisoxazol-3-yl, and pharmaceutically acceptable salts thereof for enhancing cognition in conditions such as Alzheimer's Disease, pharmaceutical compositions comprising them, their use for manufacturing medicaments and methods of treatment using them
摘要翻译：本发明提供式（I）化合物，其中R 1通常是氢或CF 3，R 2通常是氢，W 是环状胺，杂环或LYX基团，其中LY是连接部分，X通常是芳族或非芳族杂环，烷基或烷基羰基，Z通常是杂环，例如5-甲基异恶唑-3-基和药学上用于增强诸如阿尔茨海默氏病等疾病的认知的可接受的盐，包含它们的药物组合物，其用于制备药物的用途和使用它们的治疗方法

3. 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。

4. 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。

5. 发明授权

US06900209B2 Nitrogen substituted 1,2,4-triazolo[3,4-a]phthalazine derivatives for enhancing cognition 失效
标题翻译：氮取代的1,2,4-三唑并[3,4-a]酞嗪衍生物用于增强认知
公开(公告)号：US06900209B2
公开(公告)日：2005-05-31
申请号：US10432391
申请日：2001-11-22
申请人： Mark Stuart Chambers , Philip Jones , Angus Murray MacLeod , Robert James Maxey , Helen Jane Szekeres
发明人： Mark Stuart Chambers , Philip Jones , Angus Murray MacLeod , Robert James Maxey , Helen Jane Szekeres
IPC分类号： C07D487/04 , A61K31/5025 , A61P25/28
CPC分类号： C07D487/04
摘要： The present invention provides a compound of formula (I) wherein A is an optionally substituted C1-4alkylidene group or a bond, R20 and R21 are hydrogen, alkyl groups or heterocyclic groups, R1 and R2 are small substituents or hydrogen, L is O, S or substituted N, X is a 5- or 6-membered heteroaromatic ring, Y is C1-4alkylidene and Z is a 5- or 6-membered heteroaromatic ring; or a pharmaceutically acceptable salt thereof; pharmaceutical compositions comprising it; its use in therapy; its use in making medicaments for treating neurodegenerative disease and methods of using it to enhance cognition.
摘要翻译：本发明提供式（I）的化合物，其中A是任选取代的C 1-4烷基或键，R 20和R 21， / SO 2是氢，烷基或杂环基，R 1和R 2是小取代基或氢，L是O，S或取代的N，X是5 - 或6-元杂芳环，Y是C 1-4 - 亚烷基，Z是5-或6-元杂芳环; 或其药学上可接受的盐; 包含它的药物组合物; 其用于治疗; 其用于制备用于治疗神经退行性疾病的药物和使用其增强认知的方法。

6. 发明授权

US07271191B2 Pyrazole derivatives as gamma-secretase inhibitors useful in the treatment of Alzheimer's disease 失效
标题翻译：吡唑衍生物作为可用于治疗阿尔茨海默病的γ-分泌酶抑制剂
公开(公告)号：US07271191B2
公开(公告)日：2007-09-18
申请号：US10549226
申请日：2004-04-01
申请人： Michela Bettati , Mark Stuart Chambers , Peter Alan Hunt , Philip Jones , Angus Murray MacLeod , Helen Jane Szekeres , Martin Richard Teall
发明人： Michela Bettati , Mark Stuart Chambers , Peter Alan Hunt , Philip Jones , Angus Murray MacLeod , Helen Jane Szekeres , Martin Richard Teall
IPC分类号： A61K31/415 , C07D231/24 , C07D231/12
CPC分类号： C07D231/12 , C07D401/04 , C07D401/06 , C07D409/12
摘要： The compounds of formula I: inhibit gamma secretase and hence are of utility in the treatment or prevention of Alzheimer's Disease.
摘要翻译：式I化合物：抑制γ-分泌酶，因此可用于治疗或预防阿尔茨海默氏病。

7. 发明授权

US07153868B2 N-(3-(4-substituted-1-piperidinyl)-1-phenylpropyl) substituted sulfonamides as NK-3 receptor antagonists 失效
标题翻译： N-（3-（4-取代-1-哌啶基）-1-苯基丙基）取代的磺酰胺作为NK-3受体拮抗剂
公开(公告)号：US07153868B2
公开(公告)日：2006-12-26
申请号：US10417360
申请日：2003-04-16
申请人： Mark Stuart Chambers , Philip Jones , Helen Jane Szekeres
发明人： Mark Stuart Chambers , Philip Jones , Helen Jane Szekeres
IPC分类号： A61K31/445 , C07D401/06
CPC分类号： C07D401/04 , A61K31/454 , A61K31/497 , C07D211/58 , C07D401/14 , C07D409/14
摘要： The present invention provides a method of treatment of a subject suffering from a disease, such as schizophrenia, for which the administration of an NK-3 antagonist is indicated which comprises administering to that subject a therapeutically effective amount of a compound of formula I: wherein, generally, Q is R1 is benzyl, phenyl, thiophene or imidazolyl optionally substituted with C1-4alkyl or halogen, such as methyl, fluorine or bromine; R2 is hydrogen or C1-4alkyl such as methyl; R3 is phenyl; R4 is hydrogen; R5 is hydrogen or C1-6alkylcarbonyl such as methylcarbonyl; X is —SO2— or —C(O)N(R2)SO2— where R2 is preferably hydrogen; Y is a bond, CH2 or Z1 where Z1 is —N(Rf)— in which Rf is C1-6alkylcarbonyl such as ethylcarbonyl; and R6 is phenyl, pyrazolyl, pyridyl, pyrimidinyl or benzimidazolonyl optionally substituted with one or two groups chosen from C1-6alkyl and benzyl, such as methyl, ethyl and benzyl; or a pharmaceutically acceptable salt thereof.
摘要翻译：本发明提供治疗患有诸如精神分裂症的受试者的方法，所述疾病包括施用NK-3拮抗剂，其包括向该受试者施用治疗有效量的式I化合物：其中通常，Q是R 1是苄基，苯基，噻吩或任选被C 1-4烷基或卤素取代的咪唑基，例如甲基，氟或溴; R 2是氢或C 1-4烷基，例如甲基; R 3是苯基; R 4是氢; R 5是氢或C 1-6烷基羰基，例如甲基羰基; X是-SO 2 - 或-C（O）N（R 2）SO 2 - ，其中R 2 O / >优选为氢; Y是键，CH 2或Z 1，其中Z 1是-N（R f）， - 其中R 1是C 1-6烷基羰基，例如乙基羰基; R 6是苯基，吡唑基，吡啶基，嘧啶基或苯并咪唑烷基，任选地被一个或两个选自C 1-6烷基和苄基的基团取代，例如甲基，乙基和苄基; 或其药学上可接受的盐。

8. 发明授权

US06900215B2 Imidazo-pyrimidine derivatives as ligands for gaba receptors 有权
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：US06900215B2
公开(公告)日：2005-05-31
申请号：US10100797
申请日：2002-03-19
申请人： Mark Stuart Chambers , Simon Charles Goodacre , David James Hallett , Andrew Jennings , Philip Jones , Richard Thomas Lewis , Kevin William Moore , Michael Geoffrey Neil Russell , Leslie Joseph Street , Helen Jane Szekeres
发明人： Mark Stuart Chambers , Simon Charles Goodacre , David James Hallett , Andrew Jennings , Philip Jones , Richard Thomas Lewis , Kevin William Moore , Michael Geoffrey Neil Russell , Leslie Joseph Street , Helen Jane Szekeres
IPC分类号： C07D487/04 , A61K31/519 , A61P25/22
CPC分类号： C07D487/04
摘要： A class of 3-phenylimidazo[1,2-α]pyrimidine derivatives, substituted at the meta position of the phenyl ring by an optionally substituted aryl or heteroaryl group which is directly attached or bridged by an oxygen atom or a —NH— linkage, and further substituted on the phenyl ring by alkyl, trifluoromethyl, alkoxy or one or two halogen atoms, especially fluoro, 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3-苯基咪唑并[1,2-a]嘧啶衍生物，其在苯环的间位被被氧原子或-NH-键直接连接或桥连的任选取代的芳基或杂芳基取代，并且在苯环上被烷基，三氟甲基，烷氧基或一个或两个卤原子，特别是氟取代，是GABA A A受体的选择性配体，特别是对α2和/或α3具有良好的亲和力和/或其α5亚基，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。

9. 发明授权

US06730681B2 Triazolo-pyrimidine derivatives as ligands for gaba receptors 失效
标题翻译：三唑并嘧啶衍生物作为gaba受体的配体
公开(公告)号：US06730681B2
公开(公告)日：2004-05-04
申请号：US10149851
申请日：2002-06-14
申请人： Mark Stuart Chambers , Ian James Collins , Simon Charles Goodacre , David James Hallett , Philip Jones , Linda Elizabeth Keown , Robert James Maxey , Leslie Joseph Street
发明人： Mark Stuart Chambers , Ian James Collins , Simon Charles Goodacre , David James Hallett , Philip Jones , Linda Elizabeth Keown , Robert James Maxey , Leslie Joseph Street
IPC分类号： A61K31519
CPC分类号： C07D487/04
摘要： A class of substituted or 6,7-ring fused [1, 2, 3]triazolo[1,5-&agr;]-pyrimidine derivatives, possessing an optionally substituted cycloalkyl, phenyl or heteroaryl substituent at the 3-position and an amino moiety at the 5-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：一类取代或6,7环稠合的[1,2,3]三唑并[1,5-a]嘧啶衍生物，其在3-位上具有任选取代的环烷基，苯基或杂芳基取代基，氨基部分 5位是GABA A受体的选择性配体，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

10. 发明授权

US09765091B2 Tetrahydropyrazolo [3,4-b] azepine derivatives and their use as allosteric modulators of metabotropic glutamate receptors 有权
公开(公告)号：US09765091B2
公开(公告)日：2017-09-19
申请号：US13809581
申请日：2011-07-11
申请人： Christelle Bolea , Sylvain Celanire , Lam Tang , Nigel J. Liverton , Philip Jones
发明人： Christelle Bolea , Sylvain Celanire , Lam Tang , Nigel J. Liverton , Philip Jones
IPC分类号： C07D513/12 , A61K31/4162 , A61K31/429 , A61K31/55 , A61K45/06 , C07D513/04 , C07D513/14 , A61K31/433 , A61K31/4439 , A61K31/506 , A61B5/00 , A61K9/00 , A61K9/06 , A61K9/10 , A61K9/20 , A23L5/00
CPC分类号： C07D513/12 , A23L5/00 , A61B5/00 , A61K9/0019 , A61K9/0095 , A61K9/06 , A61K9/10 , A61K9/2059 , A61K31/429 , A61K31/433 , A61K31/4439 , A61K31/506 , A61K31/55 , A61K45/06 , C07D513/04 , C07D513/14 , A61K2300/00
摘要： The present invention relates to novel compounds of Formula (I), wherein M, A and Y are defined as in Formula (I); invention compounds are modulators of metabotropic glutamate receptors—subtype 4 (“mGluR4”) which are useful for the treatment or prevention of central nervous system disorders as well as other disorders modulated by mGluR4 receptors. The invention is also directed to pharmaceutical compositions and the use of such compounds in the manufacture of medicaments, as well as to the use of such compounds for the prevention and treatment of such diseases in which mGluR4 is involved.

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