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1. 发明授权

US5821261A Substituted saturated aza heterocycles as inhibitors of nitric oxide synthase 失效
标题翻译：取代的饱和杂环杂环作为一氧化氮合酶的抑制剂
公开(公告)号：US5821261A
公开(公告)日：1998-10-13
申请号：US745355
申请日：1996-11-08
申请人： Philippe L. Durette , Thomas Lanza, Jr.
发明人： Philippe L. Durette , Thomas Lanza, Jr.
IPC分类号： A61K31/401 , C07D207/16 , C07D211/06 , A01N43/40
CPC分类号： C07D207/16 , A61K31/401
摘要： Disclosed herein are compounds of Formula (I) ##STR1## and pharmaceutically acceptable salts thereof which have been found useful in the treatment of nitric oxide synthase mediated diseases and disorders, including neurodegenerative disorders, disorders of gastrointestinal motility and inflammation. These disease and disorders include hypotension, septic shock, toxic shock syndrom, hemodialysis, IL-2 therapy such as in cancer patients, cachexia, immnunosuppression such as in transplant therapy, autoimmune and/or inflammatory indications including sunburn or psoriasis and respiratory conditions such as bronchitis, asthma, and acure respiratory distress (ARDS), myocarditis, heart failure, atherosclerosis, arthritis, rheumatoid arthritis, chronic or inflammatory bowel disease, ulcerative colitis, Crohn's disease, systemic lupus erythematosis (SLE), ocular conditions such as ocular hypertension and uveitis, type 1 diabetes, insulin-dependent diabetes mellitus and cystic fibrosis. Compounds of Formula I are also useful in the treatment of hypoxia, hyperbaric oxygen convulsions and toxicity, dementia, Sydenham's chorea, Parkinson's disease, Huntington's disease, amyotrophic lateral sclerosis, multiple sclerosis, Korsakoffs disease, imbecility related to cerebral vessel disorder, ischemic brain edema, sleeping disorders, schizophrenia, depression, PMS, anxiety, drug addiction, pain, migraine, immune complex disease, as immunosupressive agents and for preventing or reversing tolerance to opiates and diazepines.
摘要翻译：本文公开了已经发现可用于治疗一氧化氮合酶介导的疾病和病症（包括神经变性疾病，胃肠蠕动和炎症疾病）的式（I）化合物及其药学上可接受的盐。这些疾病和病症包括低血压，脓毒性休克，中毒性休克综合征，血液透析，诸如癌症患者中的IL-2治疗，恶病质，移植治疗中的免疫抑制，自身免疫和/或炎性适应症，包括晒伤或牛皮癣和呼吸病症，例如支气管炎，哮喘和急性呼吸窘迫（ARDS），心肌炎，心力衰竭，动脉粥样硬化，关节炎，类风湿性关节炎，慢性或炎性肠病，溃疡性结肠炎，克罗恩病，系统性红斑狼疮（SLE），眼部疾病如眼高压和葡萄膜炎，1型糖尿病，胰岛素依赖性糖尿病和囊性纤维化。式I的化合物还可用于治疗缺氧，高压氧惊厥和毒性，痴呆，Sydenham's舞蹈病，帕金森病，亨廷顿舞蹈病，肌萎缩性侧索硬化，多发性硬化，柯萨科夫病，与脑血管障碍有关的缺血性，缺血性脑水肿，睡眠障碍，精神分裂症，抑郁症，PMS，焦虑，药物成瘾，疼痛，偏头痛，免疫复合物疾病，作为免疫抑制剂，以及用于预防或逆转对阿片剂和二氮杂类药物的耐受性。

2. 发明授权

US08071568B2 Nucleoside aryl phosphoramidates for the treatment of RNA-dependent RNA viral infection 有权
标题翻译：用于治疗RNA依赖性RNA病毒感染的核苷芳基氨基磷酸酯
公开(公告)号：US08071568B2
公开(公告)日：2011-12-06
申请号：US12520738
申请日：2007-12-28
申请人： Frank Narjes , Cristina Gardelli , Monica Donghi , Barbara Attenni , Philippe L. Durette
发明人： Frank Narjes , Cristina Gardelli , Monica Donghi , Barbara Attenni , Philippe L. Durette
IPC分类号： A61K31/70 , C07H19/10
CPC分类号： C07H19/04 , C07H19/048 , C07H19/10 , C07H19/20
摘要： The present invention provides nucleoside aryl phosphoramidates of structural formula (I) which are precursors to inhibitors of RNA-dependent RNA viral polymerase. These compounds are precursors to inhibitors of RNA-dependent RNA viral replication and are useful for the treatment of RNA-dependent RNA viral infection. They are particularly useful as precursors to inhibitors of hepatitis C virus (HCV) NS5B polymerase, as precursors to inhibitors of HCV replication, and/or for the treatment of hepatitis C infection. The invention also describes pharmaceutical compositions containing such nucleoside aryl phosphoramidates alone or in combination with other agents active against RNA-dependent RNA viral infection, in particular HCV infection. Also disclosed are methods of inhibiting RNA-dependent RNA polymerase, inhibiting RNA-dependent RNA viral replication, and/or treating RNA-dependent RNA viral infection with the nucleoside aryl phosphoramidates of the present invention. (I)
摘要翻译：本发明提供结构式（I）的核苷芳基氨基磷酸酯，其是RNA依赖性RNA病毒聚合酶抑制剂的前体。这些化合物是RNA依赖性RNA病毒复制抑制剂的前体，可用于治疗RNA依赖性RNA病毒感染。它们特别可用作丙型肝炎病毒（HCV）NS5B聚合酶抑制剂的前体，作为HCV复制抑制剂的前体和/或治疗丙型肝炎感染。本发明还描述了单独或与其它对RNA依赖性RNA病毒感染，特别是HCV感染有活性的试剂组合的含有这种核苷芳基氨基磷酸酯的药物组合物。还公开了本发明的核苷芳基氨基磷酸酯抑制RNA依赖性RNA聚合酶，抑制RNA依赖性RNA病毒复制和/或治疗RNA依赖性RNA病毒感染的方法。（一世）

3. 发明授权

US5739137A 16-substituted-4-aza-3-oxo-androstane as 5-alpha-reductase isozyme 1 inhibitors 失效
标题翻译： 16-取代-4-氮杂-3-氧代 - 雄甾烷作为5-α-还原酶同工酶1抑制剂
公开(公告)号：US5739137A
公开(公告)日：1998-04-14
申请号：US601042
申请日：1996-02-28
申请人： Philippe L. Durette , William K. Hagmann , Thomas J. Lanza, Jr. , Soumya P. Sahoo , Gary H. Rasmusson , Richard L. Tolman , Derek Von Langen
发明人： Philippe L. Durette , William K. Hagmann , Thomas J. Lanza, Jr. , Soumya P. Sahoo , Gary H. Rasmusson , Richard L. Tolman , Derek Von Langen
IPC分类号： A61K31/58 , A61P5/24 , A61P17/14 , A61P29/00 , C07J73/00
CPC分类号： C07J73/005
摘要： Compounds of formula (I) are inhibitors of the 5.alpha.-reductase 1 isozyme, and are useful alone, or in combination with a 5.alpha.-reductase 2 inhibitor, for the treatment of androgenic sensitive disorders such as acne vulgaris, seborrhea, female hirsutism, male pattern baldness, and benign prostatic hyperplasia. ##STR1##
摘要翻译： PCT No.PCT / US94 / 12071 Sec。 371日期1996年2月28日 102（e）日期1996年2月28日PCT 1994年10月21日PCT PCT。出版物WO95 / 11254 日期：1995年04月27日式（I）化合物是5α-还原酶1同功酶的抑制剂，可单独使用或与5α-还原酶2抑制剂组合用于治疗雄激素敏感性疾病如寻常痤疮，皮脂溢，女性多毛症，男性型秃发和良性前列腺增生。

4. 发明授权

US5693809A Substituted 4-aza-5.alpha.-androstan-ones as 5.alpha.-reductase inhibitors 失效
标题翻译：取代的4-氮杂-5α-雄甾烷酮作为5α-还原酶抑制剂
公开(公告)号：US5693809A
公开(公告)日：1997-12-02
申请号：US338571
申请日：1995-05-12
申请人： Philippe L. Durette , William Hagmann , Gary H. Rasmusson , Richard L. Tolman , Ihor E. Kopka , Soumya P. Sahoo , Craig K. Esser , Nathan G. Steinberg , Donald W. Graham , Bruce E. Witzel
发明人： Philippe L. Durette , William Hagmann , Gary H. Rasmusson , Richard L. Tolman , Ihor E. Kopka , Soumya P. Sahoo , Craig K. Esser , Nathan G. Steinberg , Donald W. Graham , Bruce E. Witzel
IPC分类号： C07C53/136 , C07C59/82 , C07C59/90 , C07J1/00 , C07J7/00 , C07J9/00 , C07J41/00 , C07J73/00 , C07D221/02 , A61K31/435
CPC分类号： C07J1/0022 , C07C53/136 , C07C59/82 , C07C59/90 , C07J1/0011 , C07J41/0038 , C07J7/003 , C07J7/007 , C07J73/005 , C07J9/00
摘要： Described are new 16-substituted and 7,16-disubstituted 4-aza-5.alpha.-androstan-3-ones and related compounds as 5.alpha.-reductase inhibitors.
摘要翻译：描述了新的16取代和7,16-二取代的4-氮杂-5α-雄甾烷-3-酮和相关化合物作为5α-还原酶抑制剂。

5. 发明授权

US5100880A Novel betalactam elastase inhibitors containing phosphorous acid derivatives at the 4-position of the 2-azetidinone 失效
标题翻译：含有2-氮杂环丁酮4-位的亚磷酸衍生物的新型β-内酰胺弹性蛋白酶抑制剂
公开(公告)号：US5100880A
公开(公告)日：1992-03-31
申请号：US672222
申请日：1991-03-20
申请人： Philippe L. Durette , Malcolm Maccoss
发明人： Philippe L. Durette , Malcolm Maccoss
IPC分类号： A61K31/675 , A61P29/00 , C07D205/08 , C07F9/568
CPC分类号： C07F9/568 , Y10S514/851
摘要： New substituted azetidinones of the general formula (A), which have been found to be potent elastase inhibitors and thereby useful as anti-inflammatory and antidegenerative agents, are described. ##STR1##

6. 发明授权

US5006532A Derivatives of 3-hydroxyazabenzo(beta)thiophene useful as 5-lipoxygenase inhibitors 失效
标题翻译：可用作5-脂氧合酶抑制剂的3-羟基苯并苯并（β）噻吩的衍生物
公开(公告)号：US5006532A
公开(公告)日：1991-04-09
申请号：US447989
申请日：1989-12-08
申请人： Robert K. Baker , Arsenio A. Pessolano , Kathleen M. Rupprecht , Philippe L. Durette
发明人： Robert K. Baker , Arsenio A. Pessolano , Kathleen M. Rupprecht , Philippe L. Durette
IPC分类号： C07D495/04
CPC分类号： C07D495/04
摘要： 3-Hydroxyazabenzo[b]thiophene derivatives having optionally 2-aryl, 2-aralkyl, 2-alkyl or 2-alkenyl substituents were prepared by, among other methods, ring closure of an appropriately substituted benzylthio-alkoxycarbonyl-pyridine. These compounds are found to be useful in the treatment of pain, fever, inflammation, arthritic conditions, asthma, allergic disorders, skin diseases such as psoriasis and atopic eczema, cardiovascular disorders, inflammatory diseases and other leukotriene mediated diseases.

7. 发明授权

US4925831A Aminoalkyl naphthalenediols as host resistance enhancers against viral infection 失效
标题翻译：氨基烷基萘二醇作为抗病毒感染的宿主抗性增强剂
公开(公告)号：US4925831A
公开(公告)日：1990-05-15
申请号：US60208
申请日：1987-06-11
申请人： Philippe L. Durette
发明人： Philippe L. Durette
IPC分类号： A61K31/135 , A61K31/35 , C07C215/50 , C07C217/52 , C07C217/58 , C07D309/14
CPC分类号： A61K31/135 , A61K31/35 , C07C215/50 , C07C217/52 , C07C217/58 , C07D309/14 , C07C2101/08 , C07C2101/14 , C07C2103/74
摘要： Disclosed are specific aminoalkyl naphthalenediol derivatives that enhance natural human host resistance to viral infectious organisms and particularly AIDS-related viruses. Such agents are also administered prophylactically to individuals whose resistance to infection has been specifically immunocompromised by an AIDs-related (HIV) virus.
摘要翻译：公开了特定的氨基烷基萘二醇衍生物，其增强天然人宿主对病毒感染性生物体，特别是与艾滋病相关的病毒的抗性。此类药物也预防性地施用于抗感染性被AIDs相关（HIV）病毒特异性免疫受损的个体。

8. 发明授权

US4866035A Dipeptidyl saccharides as host resistance enhancers in AIDS-immuno-compromised hosts and methods of use 失效
标题翻译：二肽类糖类作为艾滋病免疫受损宿主中的宿主抗性增强剂和使用方法
公开(公告)号：US4866035A
公开(公告)日：1989-09-12
申请号：US105056
申请日：1987-10-05
申请人： Philippe L. Durette
发明人： Philippe L. Durette
IPC分类号： A61K38/03 , C07K9/00
CPC分类号： A61K31/7004 , A61K38/03 , C07K9/005
摘要： Disclosed are specific dipeptidyl saccharide derivatives which alone, or in combination with an anti-AIDS drug, e.g. azidothymidine, provide protection against opportunistic infection in human individuals whose resistance to infection has been specifically suppressed by an AIDS-related (HIV) virus, as well as help to suppress the AIDS-related infection itself.
摘要翻译：公开了单独或与抗艾滋病药物组合的特异性二肽基糖衍生物。叠氮胸苷可以防止艾滋病相关（HIV）病毒特异性抑制感染的人群中机会性感染，有助于抑制艾滋病相关感染。

9. 发明授权

US4767766A Derivatives of 3-hydroxyazabenzo(B)thiophene useful as 5-lipoxygenase inhibitors 失效
标题翻译：可用作5-脂氧合酶抑制剂的3-羟基苯并苯并（B）噻吩的衍生物
公开(公告)号：US4767766A
公开(公告)日：1988-08-30
申请号：US8881
申请日：1987-01-30
申请人： Robert K. Baker , Kathleen M. Rupprecht , Arsenio A. Pessolano , Philippe L. Durette
发明人： Robert K. Baker , Kathleen M. Rupprecht , Arsenio A. Pessolano , Philippe L. Durette
IPC分类号： C07D495/04 , A61K31/435
CPC分类号： C07D495/04
摘要： 3-Hydroxyazabenzo[b]thiophene derivatives having optionally 2-aryl, 2-aralkyl, 2-alkyl or 2-alkenyl substituents were prepared by, among other methods, ring closure of an appropriately substituted benzylthio-alkoxycarbonyl-pyridine. These compounds are found to be useful in the treatment of pain, fever, inflammation, arthritic conditions, asthma, allergic disorders, skin diseases such as psoriasis and atopic eczema, cardiovascular disorders, inflammatory diseases and other leukotriene mediated diseases.
摘要翻译：具有任选2-芳基，2-芳烷基，2-烷基或2-烯基取代基的3-羟基氮杂苯并[b]噻吩衍生物通过其它方法闭环合适取代的苄硫基 - 烷氧基羰基 - 吡啶来制备。发现这些化合物可用于治疗疼痛，发烧，炎症，关节炎病症，哮喘，过敏性疾病，皮肤疾病如牛皮癣和特应性湿疹，心血管疾病，炎性疾病和其他白三烯介导的疾病。

10. 发明授权

US4760161A Ipoxygenase inhibitors 失效
标题翻译：加氧酶抑制剂
公开(公告)号：US4760161A
公开(公告)日：1988-07-26
申请号：US488498
申请日：1983-04-25
申请人： Philippe L. Durette , Timothy F. Gallagher
发明人： Philippe L. Durette , Timothy F. Gallagher
IPC分类号： C07C33/34 , C07C63/66 , C07C69/76
CPC分类号： C07C63/66 , C07C33/34
摘要： Compounds of the Formula I: ##STR1## and pharmaceutically acceptable salts thereof are inhibitors of leukotriene biosynthesis. These compounds inhibit lipoxygenase, thus preventing the metabolism of arachidonic acid to the leukotrienes. These compounds are thus useful in the treatment of asthma, allergic disorders, inflammation, skin diseases and certain cardiovascular disorders.
摘要翻译：式Ⅰ化合物及其药学上可接受的盐是白三烯生物合成的抑制剂。这些化合物抑制脂氧合酶，从而防止花生四烯酸向白细胞三烯的代谢。因此，这些化合物可用于治疗哮喘，过敏性疾病，炎症，皮肤疾病和某些心血管疾病。

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