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1. 发明申请

US20070066620A1 2-Heteroaryl-pyrazolo-[4,3-e]-1,2,4-triazolo-[1,5-c]-pyrimidine adenosine A2a receptor antagonists 有权
标题翻译： 2-杂芳基 - 吡唑并[4,3-e] -1,2,4-三唑并 - [1,5-c] - 嘧啶腺苷A2a受体拮抗剂
公开(公告)号：US20070066620A1
公开(公告)日：2007-03-22
申请号：US11522221
申请日：2006-09-15
申请人： Bernard Neustadt , Craig Boyle , Samuel Chackalamannil , Joel Harris , Claire Lankin , Hong Liu , Unmesh Shah , Andrew Stamford
发明人： Bernard Neustadt , Craig Boyle , Samuel Chackalamannil , Joel Harris , Claire Lankin , Hong Liu , Unmesh Shah , Andrew Stamford
IPC分类号： A61K31/519 , C07D487/14
CPC分类号： C07D487/14
摘要： Compounds having the structural formula I or a pharmaceutically acceptable salt thereof, wherein R is R1-isoxazolyl, R1-oxadiazolyl, R1-dihydrofuranyl, R1-pyrazolyl, R1-imidazolyl, R1-pyrazinyl or R1-pyrimidinyl; R1 is 1, 2 or 3 substituents selected from H, alkyl, alkoxy and halo; Z is optionally substituted-aryl, or optionally substituted-heteroaryl; are disclosed, as well as their use in the treatment of central nervous system diseases, in particular Parkinson's disease and Extra Pyramidal Syndrome, pharmaceutical compositions comprising them, and combinations with other agents.
摘要翻译：具有结构式I的化合物或其药学上可接受的盐，其中R为R 1 - 异恶唑基，R 1 - 恶二唑基，R 1 - 二氢呋喃基，R 1 - 吡唑基，R 1 - 咪唑基，R 1 - 吡嗪基或R 1 - 嘧啶基; R 1是1,2或3个选自H，烷基，烷氧基和卤素的取代基; Z是任选取代的 - 芳基或任选取代的杂芳基; 以及它们在治疗中枢神经系统疾病，特别是帕金森病和额外锥体综合征，包含它们的药物组合物以及与其它药剂的组合中的用途。

2. 发明申请

US20050239795A1 Pyrazolo-[4,3-e]-1,2,4-triazolo-[1,5-c]-pyrimidine adenosine A2a receptor antagonists 有权
标题翻译：吡唑并[4,3-e] -1,2,4-三唑并 - [1,5-c] - 嘧啶腺苷A2a受体拮抗剂
公开(公告)号：US20050239795A1
公开(公告)日：2005-10-27
申请号：US11108916
申请日：2005-04-19
申请人： Bernard Neustadt , Jinsong Hao , Hong Liu , Craig Boyle , Samuel Chackalamannil , Unmesh Shah , Andrew Stamford , Joel Harris
发明人： Bernard Neustadt , Jinsong Hao , Hong Liu , Craig Boyle , Samuel Chackalamannil , Unmesh Shah , Andrew Stamford , Joel Harris
IPC分类号： A61K31/519 , C07D487/14
CPC分类号： C07D487/14
摘要： Compounds having the structural formula I or a pharmaceutically acceptable salt thereof, wherein R is optionally substituted phenyl, furanyl, thienyl, pyridyl, pyridyl N-oxide, oxazolyl or pyrrolyl, or cycloalkenyl R1, R2, R3, R4 and R5 are H, alkyl or alkoxyalkyl; and Z is optionally substituted aryl or heteroaryl are disclosed. Also disclosed is the use of compounds of formula I in the treatment of central nervous system diseases, in particular Parkinson's disease, alone or in combination with other agents for treating Parkinson's disease, and pharmaceutical compositions comprising them.
摘要翻译：具有结构式I的化合物或其药学上可接受的盐，其中R是任选取代的苯基，呋喃基，噻吩基，吡啶基，吡啶基N-氧化物，恶唑基或吡咯基，或环烯基R 1， R 3，R 3，R 4和R 5是H，烷基或烷氧基烷基; 和Z是任选取代的芳基或杂芳基。还公开了式I化合物在治疗中枢神经系统疾病，特别是帕金森病中单独使用或与用于治疗帕金森病的其它药物组合的用途，以及包含它们的药物组合物的用途。

3. 发明申请

US20050222164A1 2-alkynyl-and 2-alkenyl-pyrazolo-[4,3-e]-1,2,4-triazolo-[1,5-c]-pyrimidine adenosine A2a receptor antagonists 有权
标题翻译： 2-炔基 - 和2-烯基 - 吡唑并[4,3-e] -1,2,4-三唑并 - [1,5-c] - 嘧啶腺苷A2a受体拮抗剂
公开(公告)号：US20050222164A1
公开(公告)日：2005-10-06
申请号：US11135261
申请日：2005-05-23
申请人： Bernard Neustadt , Jinsong Hao , Hong Liu , Craig Boyle , Samuel Chackalamannil , Unmesh Shah , Andrew Stamford
发明人： Bernard Neustadt , Jinsong Hao , Hong Liu , Craig Boyle , Samuel Chackalamannil , Unmesh Shah , Andrew Stamford
IPC分类号： A61P25/16 , C07D487/14 , A61K31/519
CPC分类号： C07D487/14
摘要： Compounds having the structural formula I or a pharmaceutically acceptable salt thereof, wherein R is R1, R2, R3, R4 and R5 are H, alkyl or alkoxyalkyl; R6 is H, alkyl, hydroxyalkyl or —CH2F; R7, R8 and R9 are H, alkyl, alkoxy, alkylthio, alkoxyalkyl, halo or —CF3; and Z is optionally substituted aryl, heteroaryl or heteroaryl-alkyl are disclosed. Also disclosed is the use of compounds of formula I in the treatment of central nervous system diseases, in particular Parkinson's disease, alone or in combination with other agents for treating Parkinson's disease, and pharmaceutical compositions comprising them.
摘要翻译：具有结构式I的化合物或其药学上可接受的盐，其中R是R 1，R 2，R 3，R 3， 4和R 5是H，烷基或烷氧基烷基; R 6是H，烷基，羟基烷基或-CH 2 F; R 7，R 8和R 9是H，烷基，烷氧基，烷硫基，烷氧基烷基，卤素或-CF 3， SUB>; 和Z是任选取代的芳基，杂芳基或杂芳基 - 烷基。还公开了式I化合物在治疗中枢神经系统疾病，特别是帕金森病中单独使用或与用于治疗帕金森病的其它药物组合的用途，以及包含它们的药物组合物的用途。

4. 发明申请

US20080070892A1 TREATING PAIN, DIABETES, AND DISORDERS OF LIPID METABOLISM 审中-公开
标题翻译：治疗脂肪代谢的疼痛，糖尿病和疾病
公开(公告)号：US20080070892A1
公开(公告)日：2008-03-20
申请号：US11854623
申请日：2007-09-13
申请人： Joel Harris , Bernard Neustadt , Stephen Sorota , Andrew Stamford , Deen Tulshian , Brian McKittrick
发明人： Joel Harris , Bernard Neustadt , Stephen Sorota , Andrew Stamford , Deen Tulshian , Brian McKittrick
IPC分类号： A61K31/439 , A61P3/06
CPC分类号： A61K31/438 , A61K31/444 , A61K31/495 , A61K31/497 , A61K31/513 , A61K45/06
摘要： Disclosed is a method of treating a disease or condition (e.g., pain, diabetes or disorders of lipid metabolism) comprising administering an azetidine derivative of the formula I selected from the group consisting of the compounds defined by Tables 1, 2, 3a, 3b, 3c, 3d and 4a.
摘要翻译：公开了治疗疾病或病症（例如，疼痛，糖尿病或脂质代谢紊乱）的方法，包括给予式I的氮杂环丁烷衍生物，其选自表1,2,3,2a，3b， 3c，3d和4a。

5. 发明申请

US20080076750A1 Azetidinone Derivatives and Methods of Use Thereof 审中-公开
标题翻译：氮杂环丁酮衍生物及其使用方法
公开(公告)号：US20080076750A1
公开(公告)日：2008-03-27
申请号：US11854738
申请日：2007-09-13
申请人： Robert Aslanian , Tin-Yau Chan , Joel Harris , Brian McKittrick , Bernard Neustadt , Anandan Palani , Tony Priestley , Elizabeth Smith , Andrew Stamford , Henry Vaccaro , Dong Xiao
发明人： Robert Aslanian , Tin-Yau Chan , Joel Harris , Brian McKittrick , Bernard Neustadt , Anandan Palani , Tony Priestley , Elizabeth Smith , Andrew Stamford , Henry Vaccaro , Dong Xiao
IPC分类号： A61K31/397 , A61P25/04 , A61P3/00
CPC分类号： A61K31/4427 , C07D471/10 , C07D519/00
摘要： The present invention relates to methods for treating or preventing a disorder of lipid metabolism, pain, diabetes, a vascular condition, demyelination or nonalcoholic fatty liver disease, comprising administering a compound having the formula or a pharmaceutically acceptable salt, solvate, ester, prodrug or stereoisomer thereof, wherein: R1 and R2 are defined in Tables 1-6 herein, and R3 is -phenyl, -4-chlorophenyl, -2-pyridyl, or -3-pyridyl.
摘要翻译：本发明涉及治疗或预防脂质代谢紊乱，疼痛，糖尿病，血管病症，脱髓鞘或非酒精性脂肪性肝病的方法，包括给予具有下式的化合物或其药学上可接受的盐，溶剂合物，酯，前药或其中：R 1和R 2在本文的表1-6中定义，R 3是 - 苯基，氯苯基，-2-吡啶基或-3-吡啶基。

6. 发明申请

US20060135526A1 Pyrazolo [1,5-A] pyrimidine adenosine A2a receptor antagonists 有权
标题翻译：吡唑并[1,5-A]嘧啶腺苷A2a受体拮抗剂
公开(公告)号：US20060135526A1
公开(公告)日：2006-06-22
申请号：US11311195
申请日：2005-12-19
申请人： Martin Clasby , Samuel Chackalamannil , Bernard Neustadt , Xiaobang Gao
发明人： Martin Clasby , Samuel Chackalamannil , Bernard Neustadt , Xiaobang Gao
IPC分类号： A61K31/519 , C07D487/04
CPC分类号： C07D487/04
摘要： Compounds having the structural formula I are disclosed, wherein A is alkylene, or optionally substituted arylene, cycloalkylene or heteroaryldiyl; X is —C(O)— or —S(O)2—; R1 is alkyl or cycloalkyl; R2 is hydrogen, halo or —CN; R3 is hydrogen or alkyl; R4 is hydrogen, alkyl, alkoxy, hydroxyalkyl, aminoalkyl-, cycloalkyl, heterocycloalkyl, heterocycloalkyl substituted by alkyl, optionally substituted arylalkyl or optionally substituted heteroarylalkyl; or R3 and R4, form an optionally substituted 5-7 membered ring, said ring optionally comprising an additional heteroatom ring member; R7 is alkyl, optionally substituted phenyl, optionally substituted heteroaryl, cycloalkyl, halo, morpholinyl, optionally substituted piperazinyl, or optionally substituted azacycloalkyl. Also disclosed is the use of the compounds in the treatment of Parkinson's disease, alone or in combination with other agents for treating Parkinson's disease, pharmaceutical compositions comprising them and kits comprising the components of the combinations.
摘要翻译：公开了具有结构式I的化合物，其中A是亚烷基或任选取代的亚芳基，亚环烷基或杂芳基二基; X是-C（O） - 或-S（O）2 - 。 R 1是烷基或环烷基; R 2是氢，卤素或-CN; R 3是氢或烷基; R 4是氢，烷基，烷氧基，羟基烷基，氨基烷基 - ，环烷基，杂环烷基，被烷基，任选取代的芳基烷基或任选取代的杂芳基烷基取代的杂环烷基; 或R 3和R 4，形成任选取代的5-7元环，所述环任选地包含另外的杂原子环成员; R 7是烷基，任选取代的苯基，任选取代的杂芳基，环烷基，卤素，吗啉基，任选取代的哌嗪基或任选取代的氮杂环烷基。还公开了化合物在治疗帕金森病中的用途，单独或与其他治疗帕金森病的药物组合，包含它们的药物组合物和包含组合组分的试剂盒的用途。

7. 发明申请

US20050113380A1 [1,2,4]-Triazole bicyclic adenosine A2a receptor antagonists 有权
标题翻译： [1,2,4] - 三唑双环腺苷A2a受体拮抗剂
公开(公告)号：US20050113380A1
公开(公告)日：2005-05-26
申请号：US10973642
申请日：2004-10-26
申请人： Bernard Neustadt , Hong Liu
发明人： Bernard Neustadt , Hong Liu
IPC分类号： A61K31/519 , A61P25/00 , A61P25/16 , A61P25/24 , A61P25/28 , C07D471/04 , C07D487/04 , A61K31/496 , A61K31/498
CPC分类号： C07D471/04 , C07D487/04
摘要： Compounds having the structural formula I wherein: n is 0, 1, 2 or 3; A is C(R1) or N; R1 and R1a are H, (C1-C6)-alkyl, halo, CN or —CF3; X is —C(O)—, —O—, —SO0-2—, or optionally substituted methylene, imino, arylene or heteroaryldiyl; Y is —O—, —SO0-2—, or optionally substituted arylene, heteroaryldiyl, or nitrogen-containing heterocycloalkyl, or with certain provisos, a bond; R is optionally substituted-aryl or heteroaryl; and R2 is optionally substituted-aryl, heteroaryl, arylalkyl or heteroarylalkyl; or R2—Y is a fused piperidinyl, substituted piperazinyl or substituted piperidinyl; their use in the treatment of Parkinson's disease, alone or in combination with other agents for treating Parkinson's disease, pharmaceutical compositions comprising them and kits comprising the components of the combinations.
摘要翻译：具有结构式I的化合物，其中：n为0,1,2或3; A是C（R 1）或N; R 1和R 2是H，（C 1 -C 6 -C 6） - 烷基，卤素，CN或 -CF 3 N 3; X是-C（O） - ， - O - ， - SO 2 - 或任选取代的亚甲基，亚氨基，亚芳基或杂芳基二基; Y是-O-，-SO 0-2 - 或任选取代的亚芳基，杂芳基二基或含氮杂环烷基，或具有一定条件的键; R是任选取代的 - 芳基或杂芳基; R 2是任选取代的 - 芳基，杂芳基，芳基烷基或杂芳基烷基; 或R 2 -Y是稠合的哌啶基，取代的哌嗪基或取代的哌啶基; 其用于治疗帕金森病，单独或与用于治疗帕金森病的其它药物组合，包含它们的药物组合物和包含组合组分的试剂盒的用途。

8. 发明申请

US20070015774A1 Quinazoline derivatives useful in cancer treatment 审中-公开
标题翻译：喹唑啉衍生物可用于癌症治疗
公开(公告)号：US20070015774A1
公开(公告)日：2007-01-18
申请号：US11486300
申请日：2006-07-13
申请人： Alan Mallams , Bimalendu Dasmahapatra , Bernard Neustadt , Mark Demma , Henry Vaccaro
发明人： Alan Mallams , Bimalendu Dasmahapatra , Bernard Neustadt , Mark Demma , Henry Vaccaro
IPC分类号： A61K31/517 , C07D409/02 , C07D403/02 , C07D405/02
CPC分类号： C07D239/90 , C07D239/94 , C07D401/12 , C07D403/12 , C07D405/12 , C07D409/12 , C07D409/14 , C07D413/12
摘要： The present invention provides compounds of Formula I (wherein R1, R2, R3, L, and X are as defined herein). or a pharmaceutically acceptable salt, solvate or ester thereof. The present invention also provides compositions comprising these compounds that are useful for treating cellular proliferative diseases, disorders associated with activity of mutants of p53, or in causing apoptosis of cancer cells.
摘要翻译：本发明提供式I化合物（其中R 1，R 2，R 3，L和X如本文所定义）。或其药学上可接受的盐，溶剂合物或酯。本发明还提供了包含这些化合物的组合物，其可用于治疗细胞增殖性疾病，与p53的突变体的活性相关的病症或引起癌细胞凋亡。

9. 发明申请

US20070032502A1 Quinazoline derivatives useful in cancer treatment 审中-公开
标题翻译：喹唑啉衍生物可用于癌症治疗
公开(公告)号：US20070032502A1
公开(公告)日：2007-02-08
申请号：US11486358
申请日：2006-07-13
申请人： Alan Mallams , Bimalendu Dasmahapatra , Bernard Neustadt , Mark Demma , Henry Vaccaro
发明人： Alan Mallams , Bimalendu Dasmahapatra , Bernard Neustadt , Mark Demma , Henry Vaccaro
IPC分类号： A61K31/517 , C07D403/02
CPC分类号： C07D239/90 , C07D239/94 , C07D401/04 , C07D401/12 , C07D401/14 , C07D403/04 , C07D403/12 , C07D405/12 , C07D409/12 , C07D409/14 , C07D413/12 , C07D413/14 , C07D417/04 , C07D417/12 , C07D471/04 , C07D471/10 , C07D471/22
摘要： The present invention provides compounds of Formula I (wherein X, m, R1, R2, R3, and R4 are as defined herein). or a pharmaceutically acceptable salt, solvate or ester thereof. The present invention also provides compositions comprising these compounds that are useful for treating cellular proliferative diseases, disorders associated with activity of mutants of p53, or in causing apoptosis of cancer cells.
摘要翻译：本发明提供式I化合物（其中X，m，R 1，R 2，R 3和R 4）如本文所定义）。或其药学上可接受的盐，溶剂合物或酯。本发明还提供了包含这些化合物的组合物，其可用于治疗细胞增殖性疾病，与p53的突变体的活性相关的病症或引起癌细胞凋亡。

10. 发明申请

US20050026932A1 Adenosine A2a receptor antagonists 有权
标题翻译：腺苷A2a受体拮抗剂
公开(公告)号：US20050026932A1
公开(公告)日：2005-02-03
申请号：US10912834
申请日：2004-08-06
申请人： Bernard Neustadt , Neil Lindo
发明人： Bernard Neustadt , Neil Lindo
IPC分类号： A61K31/505 , A61K31/519 , A61P25/08 , A61P25/16 , A61P25/24 , A61P25/28 , A61P43/00 , C07D487/14
CPC分类号： C07D487/14
摘要： Compounds having the structural formula I or a pharmaceutically acceptable salt thereof, wherein R is optionally substituted phenyl, cycloalkenyl, or heteroaryl; X is alkylene or —C(O)CH2—; Y is —N(R2)CH2CH2N(R3)—, —OCH2CH2N(R2)—, —O—, —S—, —CH2S—, —(CH2)2—NH—, or optionally substituted m and n are 2-3, and Q is nitrogen or optionally substituted carbon; and Z is optionally substituted phenyl, phenylalkyl or heteroaryl, diphenylmethyl, R6—C(O)—, R6—SO2—, R6—OC(O)—, R7—N(R8)—C(O)—, R7—N(R8)—C(S)—, phenyl-CH(OH)—, or phenyl-C(═NOR2)—; or when Q is CH, phenylamino or pyridylamino; or Z and Y together are substituted piperidinyl or substituted phenyl; and R2, R3, R6, R7, and R8 are as defined in the specification are disclosed, their use in the treatment of Parkinson's disease, alone or in combination with other agents for treating Parkinson's disease, and pharmaceutical compositions comprising them; also disclosed are a processes for preparing intermediates useful for preparing compounds of formula I.
摘要翻译：具有结构式I的化合物或其药学上可接受的盐，其中R是任选取代的苯基，环烯基或杂芳基; X是亚烷基或-C（O）CH 2 - ; Y是-N（R 2）CH 2 CH 2 N（R 3） - ，-OCH 2 CH 2 N（R 2） - ， - O - ， - S - ， - CH 2 S - ， - （CH 2）2 -NH-，或任选取代的m和n为2-3，Q为氮或任选取代的碳; 和Z是任选取代的苯基，苯基烷基或杂芳基，二苯基甲基，R 6 -C（O） - ，R 6 -SO 2 - ，R 6 -OC（O） - ，R 7 -N R 8）-C（O） - ，R 7 -N（R 8）-C（S） - ，苯基-CH（OH） - 或苯基-C（= NOR 2） - ; 或当Q为CH时，为苯基氨基或吡啶基氨基; 或Z和Y一起是取代的哌啶基或取代的苯基; 和R 2，R 3，R 6，R 7和R 8如说明书中所定义，它们用于治疗帕金森病，单独或与其他组合用于治疗帕金森病的药剂和包含它们的药物组合物; 还公开了制备可用于制备式I化合物的中间体的方法。

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