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1.发明授权3,5-di-t-butyl-4-hydroxyphenylmethylhydroxylamines and their derivatives, pharmaceutical compositions, and methods of use therefor 失效3,5-二叔丁基-4-羟基苯基甲基羟胺及其衍生物，药物组合物及其使用方法
公开(公告)号：US5393923A
公开(公告)日：1995-02-28
申请号：US135213
申请日：1993-10-12
IPC分类号： C07C239/12 , C07C259/06 , C07C271/16 , C07C275/64 , C07C335/40 , C07C335/00
CPC分类号： C07C259/06 , C07C239/12 , C07C271/16 , C07C275/64 , C07C335/40
摘要： The present invention is a novel compound which is a 3,5-di-t-butyl-4-hydroxyphenylmethylhydroxylamine or derivative thereof and a pharmaceutically acceptable acid addition or base salt thereof, pharmaceutical composition and methods of use therefor. 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.
摘要翻译： 本发明是一种3,5-二叔丁基-4-羟苯基甲基羟胺或其衍生物及其药学上可接受的酸加成盐或碱盐的新型化合物，药物组合物及其用途。 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。
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2.发明授权3,5-di-t-butyl-4-hydroxylphenylmethylhydroxylamines and their derivatives, pharmaceutical compositions, and methods of use therefor 失效3,5-二叔丁基-4-羟基苯基甲基羟胺及其衍生物，药物组合物及其使用方法
公开(公告)号：US5288896A
公开(公告)日：1994-02-22
申请号：US821103
申请日：1992-01-15
IPC分类号： C07C239/12 , C07C259/06 , C07C271/16 , C07C275/64 , C07C335/40 , C07C271/00
CPC分类号： C07C259/06 , C07C239/12 , C07C271/16 , C07C275/64 , C07C335/40
摘要： The present invention is a novel compound which is a 3,5-di-t-butyl-4-hydroxyphenylmethylhydroxylamine or derivative thereof and a pharmaceutically acceptable acid addition or base salt thereof, pharmaceutical composition and methods of use therefor. 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.
摘要翻译： 本发明是一种3,5-二叔丁基-4-羟苯基甲基羟胺或其衍生物及其药学上可接受的酸加成盐或碱盐的新型化合物，药物组合物及其用途。 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。
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公开(公告)号：US5464855A
公开(公告)日：1995-11-07
申请号：US287572
申请日：1994-08-09
申请人： Thomas Capiris , David T. Connor
发明人： Thomas Capiris , David T. Connor
IPC分类号： C07D409/12 , C07D495/04 , C07D403/12 , A61K31/41 , A61K31/44
CPC分类号： C07D409/12 , C07D495/04
摘要： Thiophene-2-carboxamidotetrazoles inhibit the Mac-1 integrin and are thus useful for treating diseases mediated by Mac-1 adhesion, including inflammatory disorders.
摘要翻译： 噻吩-2-甲酰氨基四唑抑制Mac-1整联蛋白，因此可用于治疗由Mac-1粘附介导的疾病，包括炎症性疾病。
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公开(公告)号：US4581458A
公开(公告)日：1986-04-08
申请号：US660356
申请日：1984-10-12
申请人： Jagadish C. Sircar , Thomas Capiris
发明人： Jagadish C. Sircar , Thomas Capiris
IPC分类号： C07D261/14 , C07D261/18 , C07D417/12
CPC分类号： C07D417/12 , C07D261/14 , C07D261/18
摘要： 4-Hydroxy-N-[5-[(substituted hetero)methyl]-3-isoxazolyl]-2H-1,2-benzothiazine-3-carboxamide 1,1-dioxides as agents for treating pain in mammals resulting from inflammation.
摘要翻译： 4-羟基-N- [5 - [（取代的杂）甲基] -3-异恶唑基] -2H-1,2-苯并噻嗪-3-甲酰胺1,1-二氧化物作为治疗由炎症引起的哺乳动物疼痛的药剂。
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5.发明授权
公开(公告)号：US4489077A
公开(公告)日：1984-12-18
申请号：US575411
申请日：1984-02-02
申请人： Jagadish C. Sircar , Thomas Capiris
发明人： Jagadish C. Sircar , Thomas Capiris
IPC分类号： C07D261/14 , C07D261/18 , C07D417/12 , C07D413/12 , A61K31/54 , C07D417/14
CPC分类号： C07D417/12 , C07D261/14 , C07D261/18
摘要： 4-Hydroxy-N-[5-[(substituted hetero)methyl]-3-isoxazolyl]-2H-1,2-benzothiazine-3-carboxamide 1,1-dioxides as agents for treating pain in mammals resulting from inflammation.
摘要翻译： 4-羟基-N- [5 - [（取代的杂）甲基] -3-异恶唑基] -2H-1,2-苯并噻嗪-3-甲酰胺1,1-二氧化物作为治疗由炎症引起的哺乳动物疼痛的药剂。
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公开(公告)号：US06521650B1
公开(公告)日：2003-02-18
申请号：US09509917
申请日：2000-04-04
申请人： Thomas Richard Belliotti , Justin Stephen Bryans , Thomas Capiris , David Christopher Horwell , Clare Octavia Kneen , David Juergen Wustrow
发明人： Thomas Richard Belliotti , Justin Stephen Bryans , Thomas Capiris , David Christopher Horwell , Clare Octavia Kneen , David Juergen Wustrow
IPC分类号： C07D25704
CPC分类号： C07C311/32 , C07C233/36 , C07C239/14 , C07C259/06 , C07C309/25 , C07C311/05 , C07C311/09 , C07C311/33 , C07C2601/04 , C07C2601/08 , C07C2601/14 , C07C2601/18 , C07C2602/46 , C07C2603/74 , C07D211/26 , C07D257/04 , C07D271/07 , C07D285/18 , C07D309/04 , C07D335/02 , C07D401/06 , C07D405/06 , C07D407/06 , C07D409/06 , C07D413/06 , C07D417/06 , C07D419/06 , C07F9/3808 , C07F9/383 , C07F9/59 , C07F9/6552 , C07F9/655363
摘要： Novel gamma aminobutyric acids of formula (I) are disclosed and are useful as agents in the treatment of epilepsy, faintness attacks, hypokinesia, cranial disorders, neurodegenerative disorders, depression, anxiety, panic, pain, neuropathological disorders, inflammation, and gastrointestinal damage. Processes for the preparation and intermediates useful in the preparation are also disclosed.
摘要翻译： 公开了式（I）的新型γ-氨基丁酸，并且可用作治疗癫痫，微弱发作，运动功能减退，颅内疾病，神经退行性疾病，抑郁症，焦虑，恐慌，疼痛，神经病理学障碍，炎症和胃肠损伤的药剂。 还公开了用于制备的方法和可用于制备的中间体。
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7.发明授权1-substituted-1-aminomethyl-cycloalkane derivatives (=gabapentin analogues), their preparation and their use in the treatment of neurological disorders 失效1-取代-1-氨基甲基 - 环烷烃衍生物（=加巴喷丁类似物），其制备及其在治疗神经障碍中的应用公开(公告)号：US06518289B1
公开(公告)日：2003-02-11
申请号：US09509905
申请日：2000-04-03
申请人： Justin Stephen Bryans , Thomas Capiris , David Christopher Horwell , Clare Octavia Kneen , David Juergen Wustrow
发明人： Justin Stephen Bryans , Thomas Capiris , David Christopher Horwell , Clare Octavia Kneen , David Juergen Wustrow
IPC分类号： C07D25704
CPC分类号： C07D257/04 , C07C233/36 , C07C239/14 , C07C259/06 , C07C309/25 , C07C311/05 , C07C311/09 , C07C311/33 , C07C2601/04 , C07C2601/08 , C07C2601/14 , C07C2601/18 , C07C2602/46 , C07C2603/74 , C07D211/26 , C07D271/07 , C07D285/18 , C07D309/04 , C07D335/02 , C07D401/06 , C07D405/06 , C07D409/06 , C07D413/06 , C07D417/06 , C07D419/06 , C07F9/3808 , C07F9/383 , C07F9/59 , C07F9/6552 , C07F9/655363
摘要： Novel amines of formulas (1), (1C), (1F), (1G) and (1H) or a pharmaceutical acceptable salt thereof wherein n is an integer of from 0 to 2; m is an integer of from 0 to 3; R is sulfonamide, amide, phosphonic acid, heterocycle, sulfonic acid, or hydroxamic acid; A′ is a bridged ring selected from (1), (2), (3), (4), (5) wherein is the point of attachment; Z1 to Z4 are each independently selected from hydrogen and methyl; o is an integer of from 1 to 4; and p is an integer of from 0 to 2. In formula (1) above R cannot be sulfonic acid when m is 2 and n is 1 are disclosed and are useful as agents in the treatment of epilepsy, faintness attacks, hypokinesia, cranial disorders, neurodegenerative disorders, depression, anxiety, panic, pain, neuropathological disorders, especially irritable bowel syndrome.
摘要翻译： 式（1），（1C），（1F），（1G）和（1H）的新型胺或其药学上可接受的盐，其中n为0-2的整数; m为0〜3的整数; R是磺酰胺，酰胺，膦酸，杂环，磺酸或异羟肟酸; A'是选自（1），（2），（3），（4），（5）中的桥环，其中是连接点; Z 1至Z 4各自独立地选自氢和甲基; o是1至4的整数; 并且p为0至2的整数。在式（1）中，当m为2时，R不能为磺酸，n为1，并且可用作治疗癫痫，微弱发作，运动不良，颅内疾病的药剂 ，神经变性疾病，抑郁症，焦虑症，恐慌症，疼痛，神经病理学障碍，特别是肠易激综合征。
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8.发明授权3,5-di-tertiary-butyl-4-hydroxyphenyl thiazolyl, oxazolyl, and imidazolyl methanones and related compounds as antiinflammatory agents 失效作为抗炎药的3,5-二叔丁基-4-羟基苯基噻唑啉，氧杂唑和咪唑并噻唑及相关化合物
公开(公告)号：US5086064A
公开(公告)日：1992-02-04
申请号：US646411
申请日：1991-01-31
IPC分类号： A61K31/41 , A61K31/42 , A61K31/421 , A61K31/425 , A61K31/426 , A61P29/00 , C07D231/10 , C07D231/12 , C07D231/16 , C07D233/54 , C07D233/64 , C07D233/90 , C07D261/08 , C07D261/10 , C07D261/18 , C07D263/32 , C07D263/34 , C07D275/02 , C07D277/20 , C07D277/24 , C07D277/32 , C07D277/56
CPC分类号： C07D231/12 , C07D231/16 , C07D233/64 , C07D233/90 , C07D261/08 , C07D263/32 , C07D277/24
摘要： The novel 3,5-di-tertiary-butyl-4-hydroxyphenylthiazolyl, -oxazolyl, or -imidazolyl methanones and methanone oximes of the present invention are antiinflammatory agents having activity as inhibitors of 5-lipoxygenase, cyclooxygenase or both.
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公开(公告)号：US6051605A
公开(公告)日：2000-04-18
申请号：US240949
申请日：1999-01-29
申请人： Thomas Capiris , David Thomas Connor , Steven Robert Miller , Paul Charles Unangst , Lawrence David Wise
发明人： Thomas Capiris , David Thomas Connor , Steven Robert Miller , Paul Charles Unangst , Lawrence David Wise
摘要： This invention relates to compounds that are antagonists of dopamine D4 receptors, and to methods of treating psychosis and schizophrenia using a compound that is an antagonist of dopamine D4 receptors.
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，以及使用作为多巴胺D4受体拮抗剂的化合物治疗精神病和精神分裂症的方法。
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10.发明授权3,5-di-tertiary-butyl-4-hydroxyphenyl imidazolyl methanones and related compounds as antiinflammatory agents 失效3,5-二叔丁基-4-羟基苯基咪唑基甲酮和相关化合物作为抗炎剂
公开(公告)号：US5234939A
公开(公告)日：1993-08-10
申请号：US777980
申请日：1991-10-17
IPC分类号： C07D231/12 , C07D231/16 , C07D233/54 , C07D233/90 , C07D261/08 , C07D263/32 , C07D277/24
CPC分类号： C07D231/12 , C07D231/16 , C07D233/64 , C07D233/90 , C07D261/08 , C07D263/32 , C07D277/24
摘要： The novel 3,5-di-tertiary-butyl 4-hydroxyphenylimidazolyl methanones and methanone oximes of the present invention are antiinflammatory agents having activity as inhibitors of 5-lipoxygenase, cyclooxygenase or both.
摘要翻译： 本发明的新型3,5-二叔丁基-4-羟基苯基咪唑基甲酮和甲酮肟是具有作为5-脂氧合酶抑制剂，环氧合酶或两者的活性的抗炎剂。
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