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1. 发明申请

US20020002144A1 Methods and compositions for bisubstrate inhibitors of acetyltransferases 审中-公开
标题翻译：乙酰转移酶双底物抑制剂的方法和组合物
公开(公告)号：US20020002144A1
公开(公告)日：2002-01-03
申请号：US09910588
申请日：2001-07-20
申请人： The Government of the United States of America, Department of Health & Human Services
发明人： David C. Klein , M. A.A. Namboodiri , Joan L. Weller , Jeffrey A. Kowalak , Anthony K. Ho
IPC分类号： A61K048/00 , A61K031/4045
CPC分类号： A61K31/4045 , A61K31/00 , A61K31/165
摘要： The present invention provides a method of producing a bisubstrate inhibitor in a cell, comprising introducing into the cell an alkylating derivative of an acetyl acceptor substrate for an acetyltransferase present in the cell. Further provided is a method of inhibiting the activity of an acetyltransferase in a cell, comprising introducing into the cell an alkylating derivative of an acetyl acceptor substrate for an acetyltransferase present in the cell under conditions whereby a bisubstrate inhibitor will be produced, thereby inhibiting the activity of the acetyltransferase in the cell.
摘要翻译：本发明提供了一种在细胞中制备双底物抑制剂的方法，包括向细胞中引入乙酰基受体底物的烷基化衍生物，用于存在于细胞中的乙酰转移酶。进一步提供一种抑制细胞中乙酰转移酶活性的方法，包括在存在于细胞内的乙酰基转移酶的乙酰基受体底物的烷基化衍生物中导入将产生双底物抑制剂的条件，由此抑制活性的乙酰转移酶。

2. 发明申请

US20010047016A1 Method for treating depression 失效
标题翻译：治疗抑郁症的方法
公开(公告)号：US20010047016A1
公开(公告)日：2001-11-29
申请号：US09834041
申请日：2001-04-12
发明人： Gregory Oxenkrug
IPC分类号： A61K031/4045
CPC分类号： A61K31/135 , A61K31/4045 , A61K2300/00
摘要： The present invention relates to a method and composition for the treatment of depression in a human being identified as having depression. This method comprises the administration of a therapeutically effective depression treatment amount of M-3 agonists, 5-MCA-NAT or an analog, to a human being identified as having depression. The 5-MCA-NAT and its analogs may be administered alone or in combination with other agents, e.g. Canullnull antagonists.
摘要翻译：本发明涉及用于治疗人类抑郁症的方法和组合物，其被鉴定为具有抑郁症。该方法包括向被鉴定为具有抑郁症的人施用治疗有效的抑制治疗量的M-3激动剂，5-MCA-NAT或类似物。 5-MCA-NAT及其类似物可以单独施用或与其它试剂组合施用，例如， Ca ++拮抗剂。

3. 发明申请

US20020025977A1 N-phenyl benzimidazolecarboxamide and N-phenyl indolecarboxamide derivatives 失效
标题翻译： N-苯基苯并咪唑酰胺和N-苯基吲哚甲酰胺衍生物
公开(公告)号：US20020025977A1
公开(公告)日：2002-02-28
申请号：US09928722
申请日：2001-08-13
申请人： Neurogen Corporation
发明人： Raymond Horvath , Ping Ge , Taeyoung Yoon , Alan Hutchison
IPC分类号： C07D235/14 , C07D209/14 , A61K031/4184 , A61K031/4045
CPC分类号： C07D235/14 , C07D209/14 , G01N2333/726
摘要： Disclosed are compounds of the formula: 1 or the pharmaceutically acceptable non-toxic salts thereof wherein; A is N or CH; R1 and R2 represents hydrogen or lower alkyl; G, R3, R4, R5, R6, R7 and R8 are variables defined herein. These compounds are modulators of CRF receptors and are therefore useful for treating affective disorders, anxiety, depression, eating disorders, and stress disorders in humans and other animals. Methods of treatment of such disorders and well as packaged pharmaceutical compositions are also provided. Compounds of the invention are also useful as probes for the localization of CRF receptors and as standards in assays for CRF receptor binding. Methods of using the compounds in receptor localization studies are given.
摘要翻译：公开了下式的化合物或其药学上可接受的无毒盐，其中： A是N或CH; R1和R2表示氢或低级烷基; G，R3，R4，R5，R6，R7和R8是本文定义的变量。这些化合物是CRF受体的调节剂，因此可用于治疗人类和其他动物中的情感障碍，焦虑症，抑郁症，进食障碍和应激障碍。还提供了治疗这种疾病以及包装的药物组合物的方法。本发明的化合物也可用作CRF受体定位的探针，并且作为用于CRF受体结合的测定中的标准物。给出了在受体定位研究中使用化合物的方法。

4. 发明申请

US20010020036A1 5HT1 receptor agonists and metoclopramide for the treatment of migraine 审中-公开
标题翻译： 5HT1受体激动剂和甲氧氯普胺用于治疗偏头痛
公开(公告)号：US20010020036A1
公开(公告)日：2001-09-06
申请号：US09838440
申请日：2001-04-19
发明人： George H. Sands
IPC分类号： A61K031/4045
CPC分类号： A61K45/06 , A61K31/166 , A61K31/4045 , A61K31/4196 , A61K31/445 , A61K2300/00
摘要： The present invention relates to a method of treating migraine in a mammal, including a human, by administering to the mammal a 5HT1 receptor agonist, and particularly eletriptan, in combination with metoclopramide. It also relates to pharmaceutical compositions containing a pharmaceutically acceptable carrier, a 5HT1 receptor agonist and metoclopramide.
摘要翻译：本发明涉及通过向哺乳动物施用5HT1受体激动剂，特别是依他曲坦与甲氧氯普胺组合，来治疗哺乳动物（包括人）中的偏头痛的方法。它还涉及含有药学上可接受的载体，5HT1受体激动剂和甲氧氯普胺的药物组合物。

5. 发明申请

US20020037887A1 Method for reducing intraocular pressure using indole derivatives 失效
标题翻译：使用吲哚衍生物降低眼内压的方法
公开(公告)号：US20020037887A1
公开(公告)日：2002-03-28
申请号：US09915486
申请日：2001-07-25
发明人： Jesus J. Pintor , Maria A. Peral , Ward M. Peterson , Robert Plourde JR. , Edward G. Brown , Benjamin R. Yerxa
IPC分类号： A61K031/55 , A61K031/454 , A61K031/4045 , A61K031/404
CPC分类号： A61K31/404 , A61K31/4045 , A61K31/55 , A61K45/06 , A61K2300/00
摘要： The present invention provides a method of reducing intraocular pressure by administering pharmaceutical compositions comprising indole derivatives. The pharmaceutical compositions useful in this invention comprise indole derivatives and melatonin analogs of Formulae I-IV. A preferred embodiment is a method of lowering intraocular pressure using 5-(methoxycarbonylamino)-N-acetyltryptamine (5-MCA-NAT), also known as GR 135531, which has a prolonged duration of action and greater efficacy in lowering intraocular pressure compared to melatonin. The present invention further provides a method of treating disorders associated with ocular hypertension, and a method of treating various forms of glaucoma; the method comprises administering an effective dose of a pharmacuetical composition comprising an indole derivative with or without agents commonly used to treat such disorders. 1
摘要翻译：本发明提供通过给药包含吲哚衍生物的药物组合物降低眼内压的方法。用于本发明的药物组合物包含式I-IV的吲哚衍生物和褪黑素类似物。优选的实施方案是使用5-（甲氧基羰基氨基）-N-乙酰基色胺（5-MCA-NAT）（也称为GR135531）降低眼内压的方法，其具有延长的作用时间和降低眼内压的更高功效褪黑激素本发明还提供了治疗与高眼压相关的疾病的方法和治疗各种形式的青光眼的方法; 该方法包括施用有效剂量的药物组合物，所述药物组合物包含吲哚衍生物，所述药物组合物含或不含通常用于治疗所述疾病的试剂。

6. 发明申请

US20010007877A1 NOVEL ANTI-INFECTIVES 审中-公开
标题翻译：新型抗感染药
公开(公告)号：US20010007877A1
公开(公告)日：2001-07-12
申请号：US09437683
申请日：1999-11-10
发明人： GEORGE O. BURTON , RICHARD M. KEENAN , STEVEN D. KNIGHT , LANCE H. RIDGERS
IPC分类号： C07D209/04 , A61K031/4045
CPC分类号： C07D401/06 , C07D209/08 , C07D401/12 , C07D405/04 , C07D405/06 , C07D409/06 , C07D409/12
摘要： Novel anti-infectives and methods of using them are provided.
摘要翻译：提供了新的抗感染药和使用它们的方法

7. 发明申请

US20030073731A1 Compositions and methods of the use thereof achiral analogues of CC-1065 and the duocarmycins 有权
公开(公告)号：US20030073731A1
公开(公告)日：2003-04-17
申请号：US09955062
申请日：2001-09-19
发明人： Moses Lee
IPC分类号： A61K031/44 , A61K031/4178 , A61K031/4045 , A61K031/401 , A61K031/165
CPC分类号： C07D207/416 , C07C215/76 , C07C235/38 , C07C271/28 , C07C271/30 , C07D209/42 , C07D213/64 , C07D213/69 , C07D235/24 , C07D405/12 , Y02P20/55
摘要： The present invention relates to novel achiral seco-analogues of the DNA minor groove and sequence-selective alkylating agents (null)-CC1065 and the duocarmycins, depicted as general class I, II III, IV and V: 1 wherein X is a good leaving group, such as a chloride, a bromide, an iodide, a mesylate, a tosylate, an acetate, a quaternary ammonium moiety, a mercaptan, an alkylsulfoxyl, or an alkylsulfonyl group, preferably either a chloride, a bromide, or an iodide group. R1 is a suitable minor groove binding agent to enhance the interactions of the achiral seco-cyclopropaneindole (CI) or an achiral seco-duocarmycin with specific sequences of DNA. Examples of the DNA binders are given in Table 4. The preferred DNA binders are groups A, C, D, E, F, G. H and I. R1 can also include the following: t-butoxy, benzyloxy, 9-fluorenylmethyloxy or other common protecting groups for amines wherein X is a good leaving group, such as a chloride, a bromide, an iodide, a mesylate, a tosylate, an acetate, a quaternary ammonium moiety, a mercaptan, an alkylsulfoxyl, or an alkylsulfonyl group, preferably either a chloride, a bromide, or an iodide group. R1 is a suitable minor groove binding agent to enhance the interactions of the covalently reactive achiral seco-pharmacophore with specific sequences of DNA. Examples of the DNA binders are given in Table 4. The preferred DNA binders are groups A, C, D, E, F, G, H, I, J, K and L. R2 and R3 can be hydrogen or short chain alkyl (C1-C5) groups, preferably both being hydrogen atoms. The alkyl groups may be straight chain or branched and include such groups as ethyl, propyl, butyl, pentyl and hexyl. R4 and R5 can be hydrogen atoms, short alkyl groups, trifluoromethyl moieties, and alkyloxycarbonyl groups. The preferred R4 and R5 groups are methoxycarbonyl and trifluoromethyl. R can be either a benzyl, a benzyloxycarbonyl, a hydrogen atom, a 4-nitrobenzyloxycarbonyl, or a Nnull-methylpiperazinyl-N-carbonyl group wherein X is a good leaving group, R1 is a minor groove binding agent, such as the binding units of adozelesin and duocarmycins, netropsin and bisbenzimide. R2 and R3 can be hydrogen or short-chain alkyl (C1-C5) groups. R4 and R5 can be hydrogen atoms, short alkyl groups, trifluoromethyl moieties, and alkyloxycarbonyl groups. R can be either a benzyl, a benzyloxycarbonyl, a hydrogen atom, a 4-nitrobenzyloxycarbonyl, or a Nnull-methylpiperazinyl-N-carbonyl group. The present invention is further directed to pharmaceutical compositions thereof, and as a method for treatment of cancer using the subject compounds.

8. 发明申请

US20020177546A1 Dual therapy method of treating and controlling diabetes mellitus 审中-公开
标题翻译：治疗和控制糖尿病的双重治疗方法
公开(公告)号：US20020177546A1
公开(公告)日：2002-11-28
申请号：US09828077
申请日：2001-04-06
发明人： W. Blair Geho , Hans C. Geho
IPC分类号： A61K038/28 , A61K031/4045
CPC分类号： A61K31/4045 , A61K38/28 , A61K2300/00
摘要： A dual therapy method of preventing, treating, and controlling diabetes mellitus complications is disclosed. The method comprises simultaneously treating a patient in need thereof with an effective amount of a mixture of insulin and serotonin contained in a Hepatocyte Directed Delivery system.
摘要翻译：公开了预防，治疗和控制糖尿病并发症的双重治疗方法。该方法包括用有效量的肝细胞定向递送系统中所含的胰岛素和5-羟色胺的混合物同时治疗有需要的患者。

9. 发明申请

US20020137787A1 Prevention or treatment of complications related to non-insulin dependent diabetes mellitus or type 2 diabetes mellitus 审中-公开
标题翻译：预防或治疗与非胰岛素依赖性糖尿病或2型糖尿病有关的并发症
公开(公告)号：US20020137787A1
公开(公告)日：2002-09-26
申请号：US09812410
申请日：2001-03-21
发明人： W. Blair Geho , Hans C. Geho
IPC分类号： A61K031/4045
CPC分类号： A61K31/4045
摘要： A method of preventing, controlling, or treating the complications of type 2 diabetes mellitus is disclosed. The method comprises administering serotonin or an analogue therof to the liver of a patient.
摘要翻译：公开了预防，控制或治疗2型糖尿病并发症的方法。该方法包括向患者的肝脏施用5-羟色胺或类似物。

10. 发明申请

US20020099084A1 Pharmaceutically active compounds and methods of use 失效
标题翻译：药物活性化合物和使用方法
公开(公告)号：US20020099084A1
公开(公告)日：2002-07-25
申请号：US10038178
申请日：2001-11-09
发明人： N. Laxma Reddy , Michael Maillard , David Berlove , Sharad Magar , Graham J. Durant
IPC分类号： A61K031/428 , A61K031/423 , A61K031/4045 , C07D209/16
CPC分类号： C07D209/08 , C07D209/90 , C07D209/92 , C07D215/08 , C07D215/12 , C07D221/12 , C07D223/22 , C07D225/08 , C07D231/12 , C07D233/56 , C07D249/08 , C07D265/36 , C07D277/62 , C07D279/16 , C07D281/10 , C07D401/12 , C07D403/12 , C07D405/12
摘要： The present invention relates to pharmaceutically acceptable compounds, including certain substituted indolinyl and derivatives thereof, 1,2,3,4-tetrahydroquinolinyl and derivatives thereof, 1,2,3,4-tetrahydroisoquinolinyl, benznullcdnullindolinyl and 5,6-dihydrophenanthridinyl compounds, and methods of treatment and pharmaceutical compositions that utilize or comprise one or more such compounds. Compounds of the invention are particularly useful for the treatment or prophylaxis of neurological injury and neurodegenerative disorders.
摘要翻译：本发明涉及药学上可接受的化合物，包括某些取代的二氢吲哚基及其衍生物，1,2,3,4-四氢喹啉基及其衍生物，1,2,3,4-四氢异喹啉基，苯并[cd] 二氢吩芬丁基化合物，以及使用或包含一种或多种这样的化合物的治疗方法和药物组合物。本发明的化合物特别可用于治疗或预防神经损伤和神经变性疾病。

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