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61. 发明授权

US4587258A Angiotensin-converting enzyme inhibitors 失效
标题翻译：血管紧张素转换酶抑制剂
公开(公告)号：US4587258A
公开(公告)日：1986-05-06
申请号：US635390
申请日：1984-07-30
申请人： Elijah H. Gold , Bernard R. Neustadt , Elizabeth M. Smith
发明人： Elijah H. Gold , Bernard R. Neustadt , Elizabeth M. Smith
IPC分类号： C07D209/44 , A61K38/00 , A61K38/55 , A61P9/12 , C07D209/52 , C07D215/48 , C07D225/02 , C07D267/22 , C07D339/08 , C07D491/048 , C07D491/052 , C07D491/113 , C07D495/10 , C07K1/113 , C07K5/02 , C07K5/06 , C07K14/81 , C12N9/99 , A61K31/40 , C07D209/02
CPC分类号： C07K5/0222 , C07K5/022 , A61K38/00
摘要： Novel compounds with angiotensin-converting enzyme inhibitory activity are disclosed. Such compounds are useful in the treatment of cardiovascular disorders, especially hypertension and congestive heart failure, and are useful in the treatment of glaucoma.
摘要翻译：公开了具有血管紧张素转化酶抑制活性的新型化合物。这样的化合物可用于治疗心血管疾病，特别是高血压和充血性心力衰竭，并且可用于治疗青光眼。

62. 发明授权

US4584285A Antihypertensive agents 失效
标题翻译：抗高血压药
公开(公告)号：US4584285A
公开(公告)日：1986-04-22
申请号：US651378
申请日：1984-09-17
申请人： Ronald J. Doll , Bernard R. Neustadt , Elizabeth M. Smith , Charles V. Magatti , Elijah H. Gold
发明人： Ronald J. Doll , Bernard R. Neustadt , Elizabeth M. Smith , Charles V. Magatti , Elijah H. Gold
IPC分类号： A61K38/00 , C07K5/02 , A61K37/00 , C07D209/02 , C07D209/04 , C07D209/34 , C07D209/42 , C07D209/44 , C07D209/96 , C07D215/00 , C07D217/00 , C07D285/16 , C07D409/00
CPC分类号： C07K5/0222 , A61K38/00
摘要： (Benzothiadiazine, benzamido and benzenesulfonyl)phenyl-substituted carboxyalkyl dipeptide compounds are disclosed. Compounds of this invention are useful as antihypertensive agents.
摘要翻译：（苯并噻二嗪，苯甲酰氨基和苯磺酰基）苯基取代的羧烷基二肽化合物。本发明化合物可用作抗高血压剂。

63. 发明授权

US08822480B2 Bicyclic heterocycle derivatives and use thereof as GPR119 modulators 有权
标题翻译：双环杂环衍生物及其作为GPR119调节剂的用途
公开(公告)号：US08822480B2
公开(公告)日：2014-09-02
申请号：US13003681
申请日：2009-07-15
申请人： Santhosh Francis Neelamkavil , Craig D. Boyle , Samuel Chackalamannil , William J. Greenlee , Bernard R. Neustadt , Andrew W. Stamford
发明人： Santhosh Francis Neelamkavil , Craig D. Boyle , Samuel Chackalamannil , William J. Greenlee , Bernard R. Neustadt , Andrew W. Stamford
IPC分类号： C07D519/00 , A61K31/519 , A61P13/12 , A61P3/04
CPC分类号： C07D519/00 , C07D487/04
摘要： The present invention relates to Bicyclic Heterocycle Derivatives of Formula (I), compositions comprising a Bicyclic Heterocycle Derivative, and methods of using the Bicyclic Heterocycle Derivatives for treating or preventing obesity, diabetes, a metabolic disorder, a cardiovascular disease or a disorder related to the activity of a G-protein coupled receptor (GPCR) such as GPR119 in a patient.
摘要翻译：本发明涉及式（I）的双环杂环衍生物，包含双环杂环衍生物的组合物，以及使用双环杂环衍生物治疗或预防肥胖，糖尿病，代谢紊乱，心血管疾病或与在患者中G蛋白偶联受体（GPCR）如GPR119的活性。

64. 发明申请

US20100113330A1 TETRAHYDROPYRIDO[4,3-D]PYRIMIDINONE DERIVATIVES AND METHODS OF USE THEREOF 审中-公开
标题翻译：四氢吡啶并[4,3-D]嘧啶酮衍生物及其使用方法
公开(公告)号：US20100113330A1
公开(公告)日：2010-05-06
申请号：US12594044
申请日：2008-04-17
申请人： Craig D. Boyle , Bernard R. Neustadt
发明人： Craig D. Boyle , Bernard R. Neustadt
IPC分类号： A61K31/519 , A61K38/28 , A61K38/16 , A61P3/04 , A61P3/10 , A61P3/00 , A61P9/12
CPC分类号： A61K31/522
摘要： The present invention relates to methods of using Tetrahydropyrido[4,3-d]Pyrimidinone Derivatives for treating or preventing obesity, diabetes, a metabolic disorder, a cardiovascular disease or a disorder related to the activity of GPR119 in a patient.
摘要翻译：本发明涉及使用四氢吡啶并[4,3-d]嘧啶酮衍生物治疗或预防肥胖症，糖尿病，代谢紊乱，心血管疾病或与患者中GPR119活性相关的障碍的方法。

65. 发明授权

US07041666B2 Adenosine A2a receptor antagonists 有权
标题翻译：腺苷A2a受体拮抗剂
公开(公告)号：US07041666B2
公开(公告)日：2006-05-09
申请号：US10304504
申请日：2002-11-26
申请人： Julius J. Matasi , John P. Caldwell , Deen Tulshian , Lisa S. Silverman , Bernard R. Neustadt
发明人： Julius J. Matasi , John P. Caldwell , Deen Tulshian , Lisa S. Silverman , Bernard R. Neustadt
IPC分类号： C07D487/04 , A61K31/519 , A61P25/18 , A61P25/16 , A61P25/28
CPC分类号： C07D487/04
摘要： Disclosed are compounds having the structural formula or pharmaceutically acceptable salts or solvates thereof, wherein R is optionally substituted heteroaryl, optionally substituted phenyl, cycloalkenyl, —C(═CH2)CH3, —C≡C—CH3, —CH═C(CH3)2, or —CH═CH—CH3; R2 is —W—X, —NR19(CH2)m—W—X, and —NR19CH(CH3)—W—X, or R2 is alkyl, alkenyl and —NR18R19, each optionally substituted —W—X; R3 is H, halo, alkyl, trifluoromethyl, alkoxy, alkoxyalkyl, hydroxyalkyl, alkylamino, alkylaminoalkyl, dialkylamino, dialkylaminoalkyl, aminoalkyl, aryl, heteroaryl, or CN; R18 is a bond, —CH(OH)—, —CH(CH3)—, —C(CH3)n—, —(CH2)n—or —O(CH2)n—; W is aryl or heteroaryl, each optionally substituted; X is H, NH2, or substituted amino, or X is —R18—Y-Z; and n, R19, Y and Z are as defined in the specification; pharmaceutical compositions thereof, and methods of treating stroke or central nervous system diseases by administering the compound of the present invention to a patient in need of such treatment.
摘要翻译：公开了具有结构式或其药学上可接受的盐或溶剂化物的化合物，其中R是任选取代的杂芳基，任选取代的苯基，环烯基，-C（-CH 2 CH 2）CH 3 ，-C≡C-CH 3，-CH-C（CH 3）2，或-CH-CH-CH _{3 ; R 2是-WX，-NR 19（CH 2）2 -WX和-NR O SUP CH 3（CH 3 CH 3）-WX或R 2是烷基，烯基和-NR 18 R 12， 19，每个任选取代的-WX; R 3是H，卤素，烷基，三氟甲基，烷氧基，烷氧基烷基，羟基烷基，烷基氨基，烷基氨基烷基，二烷基氨基，二烷基氨基烷基，氨基烷基，芳基，杂芳基或CN; -CH（OH） - ， - CH（CH 3） - ， - （CH 3 CH 3） - ， - （CH 3 CH 3） n - - （CH 2）n - 或 - （CH 2）n - / > - ; W是芳基或杂芳基，各自任选被取代; X是H，NH 2或取代的氨基，或X是-R 18 -Y-Z; 和n，R 19，Y和Z如说明书中所定义; 其药物组合物，以及通过将本发明化合物给予需要这种治疗的患者来治疗中风或中枢神经系统疾病的方法。}

66. 发明授权

US06391865B1 Piperazine derivatives useful as CCR5 antagonists 有权
标题翻译：哌嗪衍生物可用作CCR5拮抗剂
公开(公告)号：US06391865B1
公开(公告)日：2002-05-21
申请号：US09562814
申请日：2000-05-01
申请人： Bahige M. Baroudy , John W. Clader , Hubert B. Josien , Stuart W. McCombie , Brian A. McKittrick , Michael W. Miller , Bernard R. Neustadt , Anandan Palani , Elizabeth M. Smith , Ruo Steensma , Jayaram R. Tagat , Susan F. Vice , Eric Gilbert , Marc A. Labroli
发明人： Bahige M. Baroudy , John W. Clader , Hubert B. Josien , Stuart W. McCombie , Brian A. McKittrick , Michael W. Miller , Bernard R. Neustadt , Anandan Palani , Elizabeth M. Smith , Ruo Steensma , Jayaram R. Tagat , Susan F. Vice , Eric Gilbert , Marc A. Labroli
IPC分类号： A01N5500
CPC分类号： A61K31/496 , A61K45/06 , C07D211/58 , C07D401/06 , C07D401/10 , C07D401/12 , C07D405/12 , C07D409/06 , C07D413/06 , A61K2300/00
摘要： The use of CCR5 antagonists of the formula or a pharmaceutically acceptable salt thereof, wherein R is optionally substituted phenyl, pyridyl, thiophenyl or naphthyl; R1 is hydrogen or alkyl; R2 is substituted phenyl, substituted heteroaryl, naphthyl, fluorenyl, diphenylmethyl or optionally substituted phenyl- or heteroaryl-alkyl; R3 is hydrogen, alkyl, alkoxyalkyl, cycloalkyl, cycloalkylalkyl, or optionally substituted phenyl, phenylalkyl, naphthyl, naphthylalkyl, heteroaryl or heteroarylalkyl; R4, R5 and R7 are hydrogen or alkyl; R6 is hydrogen, alkyl or alkenyl; for the treatment of HIV, solid organ transplant rejection, graft v. host disease, arthritis, rheumatoid arthritis, inflammatory bowel disease, atopic dermatitis, psoriasis, asthma, allergies or multiple sclerosis is disclosed, as well as novel compounds, pharmaceutical compositions comprising them, and the combination of CCR5 antagonists of the invention in combination with antiviral agents useful in the treatment of HIV or agents useful in the treatment of inflammatory diseases.
摘要翻译：使用式5的CCR5拮抗剂或其药学上可接受的盐，其中R是任选取代的苯基，吡啶基，噻吩基或萘基; R 1是氢或烷基; R 2是取代的苯基，取代的杂芳基，萘基，芴基，二苯基甲基或任选取代的苯基 - R 4是氢或烷基; R 6是氢，烷基或链烯基; R 4是氢或烷基; R 3是氢，烷基或烷氧基烷基，公开了用于治疗HIV，实体器官移植排斥，移植物抗宿主病，关节炎，类风湿性关节炎，炎症性肠病，特应性皮炎，牛皮癣，哮喘，过敏或多发性硬化的新型化合物，以及包含它们的药物组合物，以及本发明的CCR5拮抗剂与可用于治疗HIV的抗病毒剂或可用于治疗炎性疾病的药剂的组合。

67. 发明授权

US06387930B1 Piperidine derivatives useful as CCR5 antagonists 有权
标题翻译：哌啶衍生物可用作CCR5拮抗剂
公开(公告)号：US06387930B1
公开(公告)日：2002-05-14
申请号：US09562815
申请日：2000-05-01
申请人： Bahige M. Baroudy , John W. Clader , Hubert B. Josien , Stuart W. McCombie , Brian A. McKittrick , Michael W. Miller , Bernard R. Neustadt , Anandan Palani , Ruo Steensma , Jayaram R. Tagat , Susan F. Vice , Mark A. Laughlin
发明人： Bahige M. Baroudy , John W. Clader , Hubert B. Josien , Stuart W. McCombie , Brian A. McKittrick , Michael W. Miller , Bernard R. Neustadt , Anandan Palani , Ruo Steensma , Jayaram R. Tagat , Susan F. Vice , Mark A. Laughlin
IPC分类号： C07D40104
CPC分类号： C07D401/14 , C07D211/58 , C07D413/14 , C07D417/14
摘要： The use of CCR5 antagonists of the formula or a pharmaceutically acceptable salt thereof, wherein X is —C(R13)2—, —C(R13)(R19)—, —C(O)—, —O—, —NH—, —N(alkyl)—, R is optionally substituted phenyl, pyridyl, thiophenyl or naphthyl; R1 is H, alkyl or alkenyl; R2 is optionally substituted phenyl, phenylalkyl, heteroaryl or heteroarylalkyl, naphthyl, fluorenyl or diphenylmethyl; R3 is optionally substituted phenyl, heteroaryl or naphthyl; R4 is H, alkyl, fluoro-alkyl, cyclopropylmethyl, —CH2CH2OH, —CH2CH2—O-alkyl, —CH2C(O)—O-alkyl, —CH2C(O)NH2, —CH2C(O)—NHalkyl or —CH2C(O)—N(alkyl)2; R19 is optionally substituted phenyl, heteroaryl or naphthyl, cycloalkyl, cycloalkylalkyl or alkoxyalkyl; and R5, R13, R14, R15 and R16 are hydrogen or alkyl for the treatment of HIV, solid organ transplant rejection, graft v. host disease, arthritis, rheumatoid arthritis, inflammatory bowel disease, atopic dermatitis, psoriasis, asthma, allergies or multiple sclerosis is disclosed, as well as novel compounds, pharmaceutical compositions comprising them, and the combination of CCR5 antagonists of the invention in combination with antiviral agents useful in the treatment of HIV or agents useful in the treatment of inflammatory diseases.
摘要翻译：使用下式的CCR5拮抗剂或其药学上可接受的盐，其中X是-C（R 13）2 - ， - C（R 13）（R 19） - ， - C（O） - ， - O - N（烷基） - ，R是任选取代的苯基，吡啶基，噻吩基或萘基; R1是H，烷基或烯基; R2是任选取代的苯基，苯基烷基，杂芳基或杂芳基烷基，萘基，芴基或二苯基甲基; R 3是任选取代的苯基，杂芳基或萘基; R4是H，烷基，氟代烷基，环丙基甲基，-CH2CH2OH，-CH2CH2-O-烷基，-CH2C（O）-O-烷基，-CH2C（O）NH2，-CH2C（O）或-CH 2 C（O）-N（烷基）2; R 19是任选取代的苯基，杂芳基或萘基，环烷基，环烷基烷基或烷氧基烷基; 和R 5，R 13，R 14，R 15和R 16是氢或烷基，用于治疗HIV，实体器官移植排斥，移植物抗宿主病，关节炎，类风湿性关节炎，炎性肠病，特应性皮炎，牛皮癣，哮喘，过敏或多发性硬化以及新化合物，包含它们的药物组合物，以及本发明的CCR5拮抗剂与可用于治疗HIV的抗病毒剂或可用于治疗炎性疾病的药剂的组合。

68. 发明授权

US06329395B1 Neuropeptide Y5 receptor antagonists 失效
标题翻译：神经肽Y5受体拮抗剂
公开(公告)号：US06329395B1
公开(公告)日：2001-12-11
申请号：US09326575
申请日：1999-06-07
申请人： Sundeep Dugar , Bernard R. Neustadt , Andrew W. Stamford , Yusheng Wu
发明人： Sundeep Dugar , Bernard R. Neustadt , Andrew W. Stamford , Yusheng Wu
IPC分类号： A61K31445
CPC分类号： C07D213/40 , C07C233/15 , C07C233/25 , C07C233/29 , C07C275/28 , C07C275/32 , C07C275/34 , C07C275/38 , C07C311/05 , C07C323/41 , C07C323/44 , C07C2601/02 , C07C2601/08 , C07C2601/14 , C07D211/58 , C07D213/38 , C07D213/74 , C07D295/135 , C07D295/15 , C07D295/215 , C07D317/72
摘要： Compounds of the formula I or a pharmaceutically acceptable salt thereof, wherein a and b are 0-2, provided that the sum is 0-3; X is —O—, —S—, —SO—, —SO2—, —CH(OR8)—, —C(O)—, —C(R23)2—, optionally substituted alkenyl, alkynyl or; R1 is optionally substituted aryl, heteroaryl, substituted amino, alkyl-OC(O)R8, aryloxyalkyl, wherein m is 1-4, or wherein d and e are 0-2; R2, R3, R4 and R5 are H, alkyl, optionally substituted cycloalkyl, halogen, —OR8, —N(R8)2, —CO2R8 or CF3; R6 and R7 are H, alkyl, alkenyl, hydroxyalkyl, aminoalkyl, alkoxy-alkyl, cycloalkyl or cycloalkylalkyl, or R6 and R7, form a 3-7-membered carbocyclic ring, or a 4-7-membered heterocyclic ring; R8 is H, alkyl, cycloalkyl, optionally substituted aryl or heteroaryl; R9 is alkyl, cycloalkyl, optionally substituted aryl or heteroaryl; R11 is H, alkyl or cycloalkyl; and R23 is R8 or halogen; are claimed, as well as additional novel compounds; also claimed are pharmaceutical compositions and methods of using said novel compounds in the treatment of eating disorders and diabetes.
摘要翻译：式I的化合物或其药学上可接受的盐，其中a和b为0-2，条件是总和为0-3; X是-O - ， - S - ， - SO - ， - SO 2 - ， - CH（OR 8 ） - ， - C（O） - ， - C（R 23）2 - ，任选取代的烯基，炔基或R 1是任选取代的芳基，杂芳基，取代的氨基，烷基-C（O）R 8，芳氧基烷基，其中m是1 -4或其中d和e为0-2; R 2，R 3，R 4和R 5为H，烷基，任选取代的环烷基，卤素，-OR 8，-N（R 8）2，-CO 2 R 8或CF 3; R 6和R 7为 H，烷基，烯基，羟基烷基，氨基烷基，烷氧基 - 烷基，环烷基或环烷基烷基，或R6和R7形成3-7元碳环或4-7元杂环; R8是H，烷基，环烷基，任选取代的芳基或杂芳基; R 9为烷基，环烷基，任选取代的芳基或杂芳基; R 11为H，烷基或环烷基; R 23为R 8或卤素; 以及其他新型化合物; 还要求的是使用所述新型化合物治疗进食障碍和糖尿病的药物组合物和方法。

69. 发明授权

US06228985B1 Derivatives of aminobenzoic and aminobiphenylcarboxylic acids useful as anti-cancer agents 失效
标题翻译：用作抗癌剂的氨基苯甲酸和氨基联苯羧酸的衍生物
公开(公告)号：US06228985B1
公开(公告)日：2001-05-08
申请号：US09082787
申请日：1998-05-21
申请人： Christine H. Blood , Bernard R. Neustadt , Elizabeth M. Smith
发明人： Christine H. Blood , Bernard R. Neustadt , Elizabeth M. Smith
IPC分类号： C07K200
CPC分类号： C07C229/38 , A61K38/00 , C07C237/36 , C07D209/18 , C07D209/20
摘要： The present invention provides compounds having the formula: wherein n is 0 or 1; R is —NH2 or wherein R1 and R2 are independently selected from the group consisting of H, alkyl, aralkyl, heteroaralkyl, carboxy, carboxyalkyl, and carbamoyl; Q is R3C(O)— or wherein R5 is selected from the group consisting of H, alkyl, aralkyl, heteroaralkyl, and carbamoylalkyl, and R3 and R4 are selected from the group consisting of H, alkyl, alkoxy, arylalkoxy, aralkyl, heteroaralkyl, and carbamoylalkyl; the Q—NH—(CH2)n— and the —C(O)R substituents of the compound of formula I are independently positioned ortho, meta, orpara relative to the carbon atoms that form the bond between the two phenyl groups to which said substituents are bound, with the proviso that said substituents are not both positioned ortho; and the Q—NH—(CH2)n and the —C(O)R substituents of the compound of formula II are positioned meta orpara to each other; or a biolabile ester thereof, or a pharmaceutically acceptable salt thereof. The compounds are useful for treating uPA- or uPAR-mediated disorders, e.g., tumor metastasis, tumor angiogenesis, restenosis, chronic inflammation, or corneal angiogenesis.
摘要翻译：本发明提供具有下式的化合物：其中n为0或1; R为-NH 2，其中R1和R2独立地选自H，烷基，芳烷基，杂芳烷基，羧基，羧基烷基和氨基甲酰基; Q为R3C （O） - 或其中R 5选自H，烷基，芳烷基，杂芳烷基和氨基甲酰基烷基，R 3和R 4选自H，烷基，烷氧基，芳基烷氧基，芳烷基，杂芳烷基和氨基甲酰基烷基; 式I化合物的Q-NH-（CH 2）n - 和-C（O）R取代基相对于形成所述取代基的两个苯基之间的键的碳原子独立地位于邻位，间位或对位条件是所述取代基不都位于邻位; 和式II化合物的Q-NH-（CH 2）n和-C（O）R取代基彼此定位在间或其生物不稳定酯或其药学上可接受的盐中。该化合物可用于治疗uPA或uPAR介导的病症，例如肿瘤转移，肿瘤血管发生，再狭窄，慢性炎症或角膜血管生成。

70. 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。

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