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1. 发明授权

US5977110A Substituted cyclohexylamines as central nervous systems agents 失效
标题翻译：取代的环己胺作为中枢神经系统药剂
公开(公告)号：US5977110A
公开(公告)日：1999-11-02
申请号：US43331
申请日：1998-03-20
申请人： Thomas R. Belliotti , Suzanne R. Kesten , Thomas A. Pugsley , David J. Wustrow
发明人： Thomas R. Belliotti , Suzanne R. Kesten , Thomas A. Pugsley , David J. Wustrow
IPC分类号： C07D213/74 , C07D235/30 , C07D239/42 , C07D239/46 , C07D239/94 , C07D241/20 , C07D277/38 , C07D277/42 , C07D277/82 , C07D401/12 , C07D403/12 , C07D417/12 , A61K31/505 , A61K31/495 , C07D403/02 , C07D403/14 , C07D417/02 , C07D417/14
CPC分类号： C07D213/74 , C07D235/30 , C07D239/42 , C07D239/47 , C07D239/94 , C07D241/20 , C07D277/42 , C07D277/82 , C07D401/12 , C07D403/12 , C07D417/12
摘要： Substituted cyclohexylamines and derivatives thereof are described, as well as methods for the preparation and pharmaceutical composition of same, which are useful as central nervous system agents and are particularly useful as dopaminergic, serotonergic, antipsychotic, and anxiolytic agents.
摘要翻译： PCT No.PCT / US96 / 13687第 371日期：1998年3月20日 102（e）1998年3月20日PCT PCT 1996年8月23日PCT公布。出版物WO97 / 11070 日期1997年3月27日描述了取代的环己胺及其衍生物，以及其制备方法及其药物组合物，其可用作中枢神经系统试剂，并且特别可用作多巴胺能，5-羟色胺能，抗精神病药和抗焦虑剂。

2. 发明授权

US06177422B1 Benzoxazinone dopamine D4 receptor antagonists 失效
标题翻译：苯并恶嗪酮多巴胺D4受体拮抗剂
公开(公告)号：US06177422B1
公开(公告)日：2001-01-23
申请号：US09180376
申请日：1998-11-04
申请人： Thomas R. Belliotti , Lawrence D. Wise , David J. Wustrow
发明人： Thomas R. Belliotti , Lawrence D. Wise , David J. Wustrow
IPC分类号： A61K31535
CPC分类号： C07D265/36
摘要： This invention relates to compounds that are antagonists of dopamine D4 receptors, to methods of treating psychosis and schizophrenia using a compound that is an antagonist of dopamine D4 receptors, and to pharmaceutically acceptable compositions that contain a dopamine D4 receptor antagonist.
摘要翻译：本发明涉及作为多巴胺D4受体的拮抗剂的化合物，使用作为多巴胺D4受体的拮抗剂的化合物治疗精神病和精神分裂症的方法以及含有多巴胺D4受体拮抗剂的药学上可接受的组合物。

3. 发明授权

US5284949A 2-substituted amino-4,6-di-tertiary-butyl-5-hydroxy-1,3-pyrimidines as antiinflammatory agents 失效
标题翻译： 2-取代的氨基-4,6-二叔丁基-5-羟基-1,3-嘧啶作为抗炎剂
公开(公告)号：US5284949A
公开(公告)日：1994-02-08
申请号：US29076
申请日：1993-03-10
申请人： Thomas R. Belliotti , David T. Connor , Catherine R. Kostlan
发明人： Thomas R. Belliotti , David T. Connor , Catherine R. Kostlan
IPC分类号： C07D239/46 , C07D403/12 , C07D417/12 , C07D239/02 , A61K31/505
CPC分类号： C07D239/47 , C07D403/12 , C07D417/12
摘要： The present invention is novel compounds which are 2-substituted amino-4,6-di-tertiarybutyl-5-hydroxy-1,3-pyrimidines and pharmaceutically acceptable acid addition or base salts thereof, pharmaceutical compositions and methods of use therefor. The invention compounds are described as having activity as inhibitors of 5-lipoxygenase and/or cyclooxygenase providing treatment of conditions advantageously affected by such inhibition including inflammation, arthritis, pain, fever and the like. Thus, the present invention is also a pharmaceutical composition or method of manufacturing a pharmaceutical composition for the use of treating the noted conditions.
摘要翻译：本发明是2-取代氨基-4,6-二叔丁基-5-羟基-1,3-嘧啶及其药学上可接受的酸加成盐或碱盐，药物组合物及其用途的新化合物。本发明化合物被描述为具有作为5-脂氧合酶抑制剂和/或环氧合酶的作用的治疗，其提供有利于受到包括炎症，关节炎，疼痛，发烧等的这种抑制影响的病症的治疗。因此，本发明还涉及一种药物组合物或制备药物组合物用于治疗使用所提到的条件的方法。

4. 发明授权

US5212189A Thiadiazole or oxadiazole analogs of fenamic acids containing substituted hydroxamate side chains as antiinflammatory agents 失效
标题翻译：含有取代的异羟肟酸侧链的灭胺酸的噻二唑或恶二唑类似物作为抗炎剂
公开(公告)号：US5212189A
公开(公告)日：1993-05-18
申请号：US809686
申请日：1991-12-17
申请人： Thomas R. Belliotti , David T. Connor , Catherine R. Kostlan
发明人： Thomas R. Belliotti , David T. Connor , Catherine R. Kostlan
IPC分类号： C07D271/10 , C07D271/113 , C07D285/12 , C07D285/125
CPC分类号： C07D271/113 , C07D285/125
摘要： The present invention is a novel compound which is a thiadiazole or oxadiazole analog of a fenamic acid having a substituted hydroxamate side chain and pharmaceutically acceptable acid addition or base salts thereof, pharmaceutical compositions and methods of use thereof. The invention compounds are now found to have activity as inhibitors of one or both of cyclooxygenase and 5-lipoxygenase providing treatment of conditions advantageously affected by such inhibition including inflammation, arthritis, pain, fever, and the like. Thus, the present invention is also a pharmaceutical composition or method of use thereof.
摘要翻译：本发明是一种新颖的化合物，它是具有取代的异羟肟酸侧链及其药学上可接受的酸加成盐或碱式盐的茴香唑的噻二唑或恶二唑类似物，药物组合物及其使用方法。现在发现本发明化合物具有作为环加氧酶和5-脂氧合酶之一或两者的抑制剂的活性，其提供有利地受到包括炎症，关节炎，疼痛，发烧等的这种抑制影响的病症的治疗。因此，本发明也是药物组合物或其使用方法。

5. 发明授权

US5356898A Substituted 4,6-di-tertiary-butyl 5-hydroxy-pyrimidines 失效
标题翻译：取代的4,6-二叔丁基5-羟基嘧啶
公开(公告)号：US5356898A
公开(公告)日：1994-10-18
申请号：US84188
申请日：1993-07-01
申请人： Thomas R. Belliotti , Catherine R. Kostlan , David T. Connor
发明人： Thomas R. Belliotti , Catherine R. Kostlan , David T. Connor
IPC分类号： A61K31/505 , A61K31/506 , A61P1/04 , A61P9/00 , A61P9/10 , A61P11/00 , A61P29/00 , A61P43/00 , C07D239/34 , C07D239/36 , C07D401/06 , C07D413/04 , C07D413/06 , C07D417/04 , C07D417/06 , C07D239/02
CPC分类号： C07D239/36 , C07D239/34 , C07D413/04 , C07D413/06 , C07D417/04 , C07D417/06 , Y02P20/55
摘要： The present invention is novel compounds which are 4,6-di-tertiary-butyl-5-hydroxy-1,3-pyrimidine substituted 1,2,4- and 1,3,4-thiadiazoles and oxadiazoles, and 1,2,4-triazoles, and pharmaceutically acceptable additions and base salts thereof, pharmaceutical compositions and methods of use therefor. The invention compounds are now found to have activity as inhibitors of 5-lipoxygenase and/or cyclooxygenase providing treatment of conditions advantageously affected by such inhibition including inflammation, arthritis, pain, fever, and particularly rheumatoid arthritis, osteoarthritis, other inflammatory conditions, psoriasis, allergic diseases, asthma, inflammatory bowel disease, GI ulcers, cardiovascular conditions, including ischemic heart disease and atherosclerosis, and ischemia-induced cell damage, particularly brain damage caused by stroke. They can also be used topically for treating acne, sunburn, psoriasis, and eczema. Also included are leukotriene mediated pulmonary, gastrointestinal, inflammatory, dermatological, and cardiovascular conditions. The disclosed compounds also have potential utility as antioxidants. The preferred use is in treating inflammatory conditions. Thus, the present invention is also a pharmaceutical composition or method of manufacturing a pharmaceutical composition for the use of treating the noted conditions.
摘要翻译： PCT No.PCT / US92 / 00442 Sec。 371日期：1993年7月1日 102（e）日期1993年7月1日PCT提交1992年1月17日PCT公布。出版物WO92 / 本发明是4,6-二叔丁基-5-羟基-1,3-嘧啶取代的1,2,4-和1,3,4-噻二唑的新化合物，以及恶二唑和1,2,4-三唑及其药学上可接受的添加剂和碱盐，药物组合物及其使用方法。现在发现本发明化合物具有作为5-脂氧合酶和/或环加氧酶的抑制剂的活性，其提供有利地受到包括炎症，关节炎，疼痛，发烧，特别是类风湿性关节炎，骨关节炎，其它炎性病症，牛皮癣，过敏性疾病，哮喘，炎症性肠病，GI溃疡，心血管疾病，包括缺血性心脏病和动脉粥样硬化，以及缺血诱导的细胞损伤，特别是脑卒中引起的脑损伤。它们也可以局部用于治疗痤疮，晒伤，牛皮癣和湿疹。还包括白三烯介导的肺，胃肠道，炎症，皮肤病学和心血管疾病。所公开的化合物还具有作为抗氧化剂的潜在用途。优选的用途是治疗炎性病症。因此，本发明也是制备用于治疗所述病症的药物组合物的药物组合物或方法。

6. 发明授权

US5187175A 2-carbonyl substituted-5-hydroxy-1, 3-pyrimidines as antiinflammatory agents 失效
标题翻译： 2-羰基取代-5-羟基-1,3-嘧啶作为抗炎剂
公开(公告)号：US5187175A
公开(公告)日：1993-02-16
申请号：US847511
申请日：1992-03-06
申请人： Thomas R. Belliotti , David T. Connor , Catherine R. Kostlan , Steven R. Miller
发明人： Thomas R. Belliotti , David T. Connor , Catherine R. Kostlan , Steven R. Miller
IPC分类号： C07D239/36 , C07D403/06 , C07D409/06 , C07D417/06 , C07F7/08
CPC分类号： C07D239/36 , C07D403/06 , C07D409/06 , C07D417/06 , C07F7/0812
摘要： The present invention is novel compounds which are 2-carbonyl substituted-5-hydroxy-1,3-pyrimidines and pharmaceutically acceptable acid addition or base salts thereof, pharmaceutical compositions and methods of use therefor. The invention compounds are now found to have activity as inhibitors of 5-lipoxygenase and/or cyclooxygenase providing treatment of conditions advantageously affected by such inhibition including inflammation, arthritis, pain, fever and the like. Thus, the present invention is also a pharmaceutical composition or method of manufacturing a pharmaceutical composition for the use of treating the noted conditions.
摘要翻译：本发明是2-羰基取代-5-羟基-1,3-嘧啶及其药学上可接受的酸加成盐或碱盐，药物组合物及其用途的新化合物。现在发现本发明化合物具有作为5-脂氧合酶抑制剂和/或环加氧酶的活性的作用，其提供有利地受到包括炎症，关节炎，疼痛，发烧等的这种抑制影响的病症的治疗。因此，本发明也是制备用于治疗所述病症的药物组合物的药物组合物或方法。

7. 发明申请

US20130029980A1 FLAVIN DERIVATIVES 审中-公开
标题翻译： FLAVIN衍生物
公开(公告)号：US20130029980A1
公开(公告)日：2013-01-31
申请号：US13640054
申请日：2011-04-06
申请人： Philip D. G. Coish , Brian R. Dixon , David Osterman , Paul Adrian Aristoff , Manuel Navia , Frank Sciavolino , Stephanie Avola , Nick Baboulas , Thomas R. Belliotti , Angelica Bello , Judd Berman , Robert A. Chrusciel , Bruce R. Evans , Harpreet Kaur , David Moon , Vinh Pham , Andrew Roughton , Phil Wickens , Jeffrey Wilson , Heinrich J. Schostarez
发明人： Philip D. G. Coish , Brian R. Dixon , David Osterman , Paul Adrian Aristoff , Manuel Navia , Frank Sciavolino , Stephanie Avola , Nick Baboulas , Thomas R. Belliotti , Angelica Bello , Judd Berman , Robert A. Chrusciel , Bruce R. Evans , Harpreet Kaur , David Moon , Vinh Pham , Andrew Roughton , Phil Wickens , Jeffrey Wilson , Heinrich J. Schostarez
IPC分类号： C07D487/04 , A61P31/04 , A61K31/5377 , A61K31/519 , C07D491/147
CPC分类号： A01N43/90 , C07D475/14
摘要： The present invention relates novel flavin derivatives, their use and compositions for use as riboswitch ligands and/or anti-infectives.
摘要翻译：本发明涉及新的黄素衍生物，其用途和用作核糖开关配体和/或抗感染剂的组合物。

8. 发明申请

US20120295903A1 FLAVIN DERIVATIVES 审中-公开
标题翻译： FLAVIN衍生物
公开(公告)号：US20120295903A1
公开(公告)日：2012-11-22
申请号：US13381809
申请日：2010-06-30
申请人： Kenneth F. Blount , Philip D.G. Coish , Brian R. Dixon , Jayhyuk Myung , David Osterman , Phil Wickens , Stephanie Avola , Nick Baboulas , Angelica Bello , Judd Berman , Harpreet Kaur , David Moon , Vinh Pham , Andrew Roughton , Jeffrey Wilson , Jeffrey A. Leiby , Dennis Underwood , Paul Adrian Aristoff , Heinrich J. Schostarez , Robert A. Chrusciel , Thomas R. Belliotti , Bruce R. Evans , Frank C. Sciavolino , Manuel A. Navia
发明人： Kenneth F. Blount , Philip D.G. Coish , Brian R. Dixon , Jayhyuk Myung , David Osterman , Phil Wickens , Stephanie Avola , Nick Baboulas , Angelica Bello , Judd Berman , Harpreet Kaur , David Moon , Vinh Pham , Andrew Roughton , Jeffrey Wilson , Jeffrey A. Leiby , Dennis Underwood , Paul Adrian Aristoff , Heinrich J. Schostarez , Robert A. Chrusciel , Thomas R. Belliotti , Bruce R. Evans , Frank C. Sciavolino , Manuel A. Navia
IPC分类号： C07D487/04 , A01P1/00 , A61K31/5377 , A61P31/04 , A61K31/525 , A01N43/90
CPC分类号： C07D487/04
摘要： The present invention relates novel flavin derivatives and other flavin derivatives, their use and compositions for use as riboswitch ligands and/or anti-infectives. The invention also provides method of making novel flavin derivatives.
摘要翻译：本发明涉及新的黄素衍生物和其它黄素衍生物，其用途和用作核糖开关配体和/或抗感染剂的组合物。本发明还提供了制备新型黄素衍生物的方法。

9. 发明申请

US20120058989A1 ANTIBACTERIAL FLUOROQUINOLONE ANALOGS 审中-公开
标题翻译：抗生素荧光素类似物
公开(公告)号：US20120058989A1
公开(公告)日：2012-03-08
申请号：US13082269
申请日：2011-04-07
申请人： Allan S. Wagman , Heinz E. Moser , Glenn A. McEnroe , James B. Aggen , Martin S. Linsell , Adam A. Goldblum , John H. Griffin , Lloyd J. Simons , Thomas R. Belliotti , Christina R. Harris , Toni-Jo Poel , Michael J. Melnick , Ricky D. Gaston
发明人： Allan S. Wagman , Heinz E. Moser , Glenn A. McEnroe , James B. Aggen , Martin S. Linsell , Adam A. Goldblum , John H. Griffin , Lloyd J. Simons , Thomas R. Belliotti , Christina R. Harris , Toni-Jo Poel , Michael J. Melnick , Ricky D. Gaston
IPC分类号： A61K31/553 , A61P31/04 , C07D498/14 , C07D471/14 , A61K31/55 , A61K31/5517
CPC分类号： C07D471/14 , C07D498/14 , C07D513/14
摘要： Compounds having antibacterial activity are disclosed. The compounds have the following structure (I): including stereoisomers, pharmaceutically acceptable salts and prodrugs thereof, wherein A, B, D, E, G, R1, R2, R3, R4, R5, R6 and R7 are as defined herein. Methods associated with preparation and use of such compounds, as well as pharmaceutical compositions comprising such compounds, are also disclosed.
摘要翻译：公开了具有抗菌活性的化合物。该化合物具有以下结构（I）：包括其立体异构体，药学上可接受的盐和前药，其中A，B，D，E，G，R 1，R 2，R 3，R 4，R 5，R 6和R 7如本文所定义。还公开了与这种化合物的制备和使用相关的方法以及包含这些化合物的药物组合物。

10. 发明授权

US5143929A 2-substituted thiazolidinone, oxazolidinone, and imidazolidinone derivatives of fenamates as antiinflammatory agents 失效
标题翻译： 2-取代噻唑烷酮，恶唑烷酮和咪唑烷酮的咪唑烷酮衍生物作为抗炎剂
公开(公告)号：US5143929A
公开(公告)日：1992-09-01
申请号：US697822
申请日：1991-05-09
申请人： Thomas R. Belliotti , Diane H. Boschelli , David T. Connor , Catherine R. Kostlan
发明人： Thomas R. Belliotti , Diane H. Boschelli , David T. Connor , Catherine R. Kostlan
IPC分类号： C07D277/34 , C07D277/36 , C07D277/54
CPC分类号： C07D277/36 , C07D277/34 , C07D277/54
摘要： The present invention is for selected novel compounds which are 2-substituted thiazolidinone, oxazolidinone, and imidazolidinone derivatives of fenamates, as well as pharmaceutical compositions and methods of use thereof. These compounds exhibit activity useful in treating allergies and inflammation.
摘要翻译：本发明涉及选择性的新型化合物，其为2-取代噻唑烷酮，恶唑烷酮和咪唑烷酮的咪唑烷酮衍生物，以及药物组合物及其使用方法。这些化合物表现出用于治疗过敏和炎症的活性。

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