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71. 发明授权

US5407960A Mercaptocycloacyl aminoacid endopeptidase inhibitors 失效
标题翻译：巯基环酰基氨基酸内肽酶抑制剂
公开(公告)号：US5407960A
公开(公告)日：1995-04-18
申请号：US859727
申请日：1992-06-11
申请人： Bernard R. Neustadt
发明人： Bernard R. Neustadt
IPC分类号： A61K31/40 , A61K38/22 , A61K38/55 , C07C323/60 , C07C327/32 , A01N37/18
CPC分类号： C07C327/32 , A61K31/40 , A61K38/2242 , A61K38/556 , C07C323/60
摘要： Mercaptocycloacyl aminoacid inhibitors of endopeptidase of the formula ##STR1## or a pharmaceutically acceptable salt thereof, alone or in combination with an ACE inhibitor or an ANF, in the treatment of cardiovascular disorders such as hypertension, congestive heart failure, edema and renal insufficiency, and treatment of nephrotoxicity pain conditions, and pharmaceutical compositions containing said compounds are disclosed.
摘要翻译： PCT No.PCT / US90 / 07353 Sec。 371日期：1992年6月11日 102（e）日期1992年6月11日PCT 1990年12月20日PCT PCT。公开号WO91 / 09840 日期1991年7月11日。式IMAGF的内肽酶或其药学上可接受的盐单独或与ACE抑制剂或ANF联合用于治疗心血管疾病如高血压，充血性心力衰竭中的巯基环酰基氨基酸抑制剂，水肿和肾功能不全以及肾毒性疼痛病症的治疗，以及含有所述化合物的药物组合物。

72. 发明授权

US5075302A Mercaptoacyl aminolactam endopeptidase inhibitors 失效
标题翻译： MERCAPTOACYL AMINOLACTAM内切酶抑制剂
公开(公告)号：US5075302A
公开(公告)日：1991-12-24
申请号：US491148
申请日：1990-03-09
申请人： Bernard R. Neustadt
发明人： Bernard R. Neustadt
IPC分类号： A61K31/395 , A61K31/40 , A61K31/4015 , A61K31/445 , A61K31/451 , A61K31/55 , A61K38/22 , A61K38/55 , A61K45/06 , A61P3/00 , A61P9/00 , A61P9/12 , A61P13/02 , A61P15/00 , A61P43/00 , C07D207/26 , C07D207/273 , C07D211/76 , C07D223/10 , C07D223/12 , C07D225/02 , C12N9/99
CPC分类号： C07D211/76 , C07D223/12
摘要： Mercaptoacyl aminolactam inhibitors of endopeptidases of the formula ##STR1## wherein Y is -(CHR.sup.5).sub.n (CR.sup.3 R.sup.4)- or -(CR.sup.3 R.sup.4).sub.p X(CR.sup.3 R.sup.4).sub.q -,wherein two substituents selected from the group consisting of R.sup.3, R.sup.4 and R.sup.5, can form a benzene, cyclopentane or cyclohexane ring;X is -O-, -S-, -SO- or -SO.sub.2 -;Q is hydrogen or R.sup.6 CO-;m is 1 or 2;n is 1, 2, 3 or 4;p is 1 or 2;q is 2 or 3;R.sup.1 is lower alkyl, aryl or heteroaryl;R.sup.2 is hydrogen, lower alkyl, hydroxylower alkyl, lower alkoxylower alkyl, aryllower alkyl or heteroaryllower alkyl;R.sup.3 and R.sup.4 are independently hydrogen, lower alkyl, aryllower alkyl or heteroaryllower alkyl;R.sup.5 is hydrogen, lower alkyl, aryllower alkyl, heteroaryllower alkyl, hydroxy, lower alkoxy, mercapto, or lower alkylthio; and R.sup.6 is lower alkyl, aryl or heteroaryl, use of the compounds, alone or in combination with an ACE inhibitor or an ANF, in the treatment of cardiovascular disorders such as hypertension, congestive heart failure, edema and renal insufficiency, use of the compounds in the treatment of pain conditions, and pharmaceutical compositions containing said compounds are disclosed.
摘要翻译：其中Y是 - （CHR5）n（CR3R4） - 或 - （CR3R4）pX（CR3R4）q-的式（III）的内肽酶的巯基酰基内酰胺抑制剂，其中两个选自R3，R4和R5的取代基，可形成苯，环戊烷或环己烷环; X是-O - ， - S - ， - SO-或-SO 2 - ; Q是氢或R6CO-; m为1或2; n为1,2,3或4; p为1或2; q为2或3; R1是低级烷基，芳基或杂芳基; R2是氢，低级烷基，羟基低级烷基，低级烷氧基低级烷基，芳基低级烷基或杂芳基低级烷基; R3和R4独立地是氢，低级烷基，芳基低级烷基或杂芳基低级烷基; R5是氢，低级烷基，芳基低级烷基，杂芳基低级烷基，羟基，低级烷氧基，巯基或低级烷硫基; R6为低级烷基，芳基或杂芳基，单独使用或与ACE抑制剂或ANF组合用于治疗心血管疾病如高血压，充血性心力衰竭，水肿和肾功能不全的化合物，使用该化合物在治疗疼痛状况时，公开了含有所述化合物的药物组合物。

73. 发明授权

US4199597A Omega-(4-polyfluoro-2-hydroxy-2-propyl)-2,3,6-substituted-phenoxy and phenylthio)alkanoic acids and compounds related thereto 失效
标题翻译： ω-（4-多氟-2-羟基-2-丙基）-2,3,6-取代苯氧基和苯硫基）链烷酸及其相关化合物
公开(公告)号：US4199597A
公开(公告)日：1980-04-22
申请号：US35963
申请日：1979-05-04
申请人： Bernard R. Neustadt , Elijah H. Gold
发明人： Bernard R. Neustadt , Elijah H. Gold
IPC分类号： C07C59/68 , C07C59/70 , C07C317/44 , C07C323/52 , A61K31/235 , C07C101/72 , C07C147/13
CPC分类号： C07C59/68 , C07C317/44 , C07C323/52 , C07C59/70
摘要： Omega-[4-(polyfluoro-2-hydroxy-2-propyl)-2,3,6-substituted-phenoxy and phenylthio]alkanoic acids and compounds related thereto having antihypertensive activity are preparable by reaction of the appropriate 2,3,6-substituted-4-(polyfluoro-2-hydroxy-2-propyl)phenol or thiophenol with an alkyl ester of a bromoalkanoic acid, followed by hydrolysis to the free acid.
摘要翻译： ω-[4-（多氟-2-羟基-2-丙基）-2,3,6-取代苯氧基和苯硫基]链烷酸及其具有抗高血压活性的化合物可通过合适的2,3,6 - 取代的4-（多氟-2-羟基-2-丙基）苯酚或苯硫酚与溴烷酸的烷基酯反应，然后水解成游离酸。

74. 发明授权

US08722882B2 Pyrimidine derivatives as GPCR modulators for use in the treatment of obesity and diabetes 有权
标题翻译：嘧啶衍生物作为用于治疗肥胖和糖尿病的GPCR调节剂
公开(公告)号：US08722882B2
公开(公告)日：2014-05-13
申请号：US13141227
申请日：2009-12-21
申请人： Bernard R. Neustadt , Andrew Stamford , Jinsong Hao , Charles Lee Jayne , Yan Xia
发明人： Bernard R. Neustadt , Andrew Stamford , Jinsong Hao , Charles Lee Jayne , Yan Xia
IPC分类号： C07D401/12 , C07D401/14 , C07D471/08 , A61K31/506 , A61P3/04 , A61P3/10
CPC分类号： C07D401/14 , C07D401/12 , C07D471/08 , C07D498/08
摘要： The present invention relates to Pyriraidine Derivatives of formula (I), compositions comprising a Pyrimidine Derivative, and methods of using the Pyrimidine Derivatives for treating or preventing obesity, diabetes, a diabetic complication, a metabolic disorder, a cardiovascular disease or a disorder related to the activity of a G protein-coupled receptor (GPCR) in a patient.
摘要翻译：本发明涉及式（I）的嘧啶衍生物，包含嘧啶衍生物的组合物，以及使用嘧啶衍生物治疗或预防肥胖症，糖尿病，糖尿病并发症，代谢障碍，心血管疾病或与 G蛋白偶联受体（GPCR）在患者体内的活性。

75. 再颁专利

USRE44205E1 Adenosine A2a receptor antagonists 有权
公开(公告)号：USRE44205E1
公开(公告)日：2013-05-07
申请号：US13441140
申请日：2012-04-06
申请人： Bernard R. Neustadt , Neil Lindo , William J. Greenlee , Deen Tulshian , Lisa S. Silverman , Yan Xia , Craig D. Boyle , Samuel Chackalamannil
发明人： Bernard R. Neustadt , Neil Lindo , William J. Greenlee , Deen Tulshian , Lisa S. Silverman , Yan Xia , Craig D. Boyle , Samuel Chackalamannil
IPC分类号： C07D471/04 , C07D471/22 , C07D487/04
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(R)3)—, —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.

76. 发明授权

US08415353B2 Amino-quinoxaline and amino-quinoline compounds for use as adenosine A2a receptor antagonists 有权
标题翻译：用作腺苷A2a受体拮抗剂的氨基喹喔啉和氨基 - 喹啉化合物
公开(公告)号：US08415353B2
公开(公告)日：2013-04-09
申请号：US12920928
申请日：2009-03-03
申请人： Joel M. Harris , Bernard R. Neustadt , Hong Liu , Jinsong Hao , Andrew W. Stamford
发明人： Joel M. Harris , Bernard R. Neustadt , Hong Liu , Jinsong Hao , Andrew W. Stamford
IPC分类号： A61K31/495
CPC分类号： C07D241/44 , C07D401/12 , C07D403/04 , C07D405/12 , C07D413/04 , C07D417/04 , C07D417/12
摘要： Compounds of the Formula (I), where W represents CH or N; and Q represents —CN, —C(═NOH)NH2, —CONHR1 or various herein described heterocyclic radicals; as well as pharmaceutically acceptable salts, solvates, esters and prodrugs thereof are adenosine A2a receptor antagonists and, therefore, are useful in the treatment of central nervous system diseases, in particular Parkinson's disease.
摘要翻译：式（I）的化合物，其中W表示CH或N; 和Q表示-CN，-C（= NOOH）NH 2，-CONHR1或本文所述的各种杂环基; 以及其药学上可接受的盐，溶剂合物，酯和前药是腺苷A2a受体拮抗剂，因此可用于治疗中枢神经系统疾病，特别是帕金森病。

77. 发明申请

US20120040975A1 BRIDGED BICYCLIC HETEROCYCLE DERIVATIVES AND METHODS OF USE THEREOF 审中-公开
标题翻译：桥联双环杂环衍生物及其使用方法
公开(公告)号：US20120040975A1
公开(公告)日：2012-02-16
申请号：US13260950
申请日：2010-04-01
申请人： Santhosh Francis Neelamkavil , Bernard R. Neustadt , Andrew Stamford , Yan Xia , Joel M. Harris , Craig D. Boyle , Samuel Chackalamannil , Dipshikha Biswas , Hong Liu , Jinsong Hao , Claire M. Lankin , Unmesh Shah
发明人： Santhosh Francis Neelamkavil , Bernard R. Neustadt , Andrew Stamford , Yan Xia , Joel M. Harris , Craig D. Boyle , Samuel Chackalamannil , Dipshikha Biswas , Hong Liu , Jinsong Hao , Claire M. Lankin , Unmesh Shah
IPC分类号： A61K31/537 , C07D401/12 , C07D491/08 , A61P3/00 , A61K31/506 , C07D487/08 , A61P3/10 , A61P3/04 , C07D451/06 , C07D498/08
CPC分类号： C07D498/08 , C07D401/12 , C07D451/02 , C07D471/08 , C07D487/08 , C07D491/08 , C07D491/113 , C07D495/08
摘要： The present invention relates to Bridged Bicyclic Heterocycle Derivatives, compositions comprising a Bridged Bicyclic Heterocycle Derivative, and methods of using the Bridged Bicyclic Heterocycle Derivatives for treating or preventing obesity, diabetes, a metabolic disorder, a cardiovascular disease or a disorder related to the activity of a GPCR in a patient.
摘要翻译：本发明涉及桥连双环杂环衍生物，包含桥连双环杂环衍生物的组合物和使用桥连双环杂环衍生物用于治疗或预防肥胖，糖尿病，代谢障碍，心血管疾病或与一名患者的GPCR。

78. 发明授权

US07790474B1 p53 modulators 失效
标题翻译： p53调节剂
公开(公告)号：US07790474B1
公开(公告)日：2010-09-07
申请号：US11487014
申请日：2006-07-14
申请人： Bimalendu Dasmahapatra , Bernard R. Neustadt , Mark Demma , Alan K. Mallams , Henry A. Vaccaro , Jonathan A. Pachter
发明人： Bimalendu Dasmahapatra , Bernard R. Neustadt , Mark Demma , Alan K. Mallams , Henry A. Vaccaro , Jonathan A. Pachter
IPC分类号： G01N33/536
CPC分类号： G01N33/5011 , G01N2333/4748
摘要： The present invention provides compositions as well as methods for identifying compositions useful for treating or preventing cancer.
摘要翻译：本发明提供组合物以及用于鉴定可用于治疗或预防癌症的组合物的方法。

79. 发明申请

US20100190687A1 PYRIMIDINONE DERIVATIVES AND METHODS OF USE THEREOF 审中-公开
标题翻译：吡咯烷酮衍生物及其使用方法
公开(公告)号：US20100190687A1
公开(公告)日：2010-07-29
申请号：US12596341
申请日：2008-04-17
申请人： Craig D. Boyle , Santhosh Francis Neelamkavil , Samuel Chackalamannil , Bernard R. Neustadt , Jinsong Hao , Unmesh G. Shah , Joel M. Harris , Hong Liu , Andrew W. Stamford
发明人： Craig D. Boyle , Santhosh Francis Neelamkavil , Samuel Chackalamannil , Bernard R. Neustadt , Jinsong Hao , Unmesh G. Shah , Joel M. Harris , Hong Liu , Andrew W. Stamford
IPC分类号： A61K38/28 , C07D487/04 , A61K31/519 , A61K31/55 , A61K38/22 , A61P3/10 , A61P3/04
CPC分类号： C07D401/04 , C07D487/04
摘要： The present invention relates to Pyrimidinone Derivatives, compositions comprising a Pyrimidinone Derivative, and methods of using the Pyrimidinone Derivatives for treating or preventing obesity, diabetes, a metabolic disorder, a cardiovascular disease or a disorder related to the activity of G protein-coupled receptor 119 (“GPR119”) in a patient.
摘要翻译：本发明涉及嘧啶酮衍生物，包含嘧啶酮衍生物的组合物，以及使用嘧啶酮衍生物治疗或预防与G蛋白偶联受体119的活性相关的肥胖症，糖尿病，代谢紊乱，心血管疾病或病症的方法（“GPR119”）。

80. 发明授权

US07709492B2 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：US07709492B2
公开(公告)日：2010-05-04
申请号：US11108916
申请日：2005-04-19
申请人： Bernard R. Neustadt , Jinsong Hao , Hong Liu , Craig D. Boyle , Samuel Chackalamannil , Unmesh G. Shah , Andrew Stamford , Joel M. Harris
发明人： Bernard R. Neustadt , Jinsong Hao , Hong Liu , Craig D. Boyle , Samuel Chackalamannil , Unmesh G. Shah , Andrew Stamford , Joel M. Harris
IPC分类号： A01N43/54 , A61K31/505 , C07D239/00 , C07D487/08
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R1，R2，R3，R4和R5是H，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。

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