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公开(公告)号：US4514414A
公开(公告)日：1985-04-30
申请号：US436232
申请日：1982-10-25
IPC分类号： C07D207/08 , A61K31/40
CPC分类号： C07D207/08
摘要： N-Substituted pyrrolidineacetic acids and their esters, useful as inhibitors of GABA uptake, are prepared by reacting an appropriate N-alkylating derivative with an esters of an N-unsubstituted pyrrolidineacetic acid followed by hydrolysis of the ester.
摘要翻译： 通过使适当的N-烷基化衍生物与N-未取代的吡咯烷基乙酸的酯反应，随后水解该酯而制备N-取代的吡咯烷酸及其酯，其可用作GABA吸收的抑制剂。
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2.发明授权Inhibition of GABA uptake by N-substituted azaheterocyclic carboxylic acids and their esters 失效通过N-取代的氮杂环羧酸及其酯抑制GABA吸收
公开(公告)号：US4383999A
公开(公告)日：1983-05-17
申请号：US372504
申请日：1982-04-28
IPC分类号： C07C17/16 , C07C17/26 , C07C43/178 , C07C45/00 , C07D211/34 , C07D211/60 , C07D211/78 , A61K31/455 , A61K31/445
CPC分类号： C07C17/2632 , C07C43/1782 , C07C45/004 , C07D211/34 , C07D211/60 , C07D211/78 , C07C2101/14
摘要： N-Substituted azaheterocyclic carboxylic acids and their esters, useful as inhibitors of GABA uptake, are prepared by reacting an appropriate N-alkylating derivative with an ester of an N-unsubstituted azaheterocyclic carboxylic acid followed by hydrolysis of the ester.
摘要翻译： 通过使适当的N-烷基化衍生物与N-未取代的氮杂杂环羧酸的酯反应，然后水解酯来制备可用作GABA摄取抑制剂的N-取代的氮杂环羧酸及其酯。
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公开(公告)号：US06489339B1
公开(公告)日：2002-12-03
申请号：US09762459
申请日：2001-02-07
IPC分类号： A61K3147
CPC分类号： C07C279/14
摘要： A compound according to Formula (I): wherein: A represents C1-4 alkylene, unsubstituted or optionally substituted by C1-4 alkyl or aryl; or A forms a 5-8 membered fused aliphatic ring with the adjacent phenyl ring; m is an integer from 1 to 3; each R1 is independently selected form the group consisting of halo, C1-4 alkyl, methanesulfonyl, alkoxy, nitrile, dimethylamine, methylenedioxy and CF3; and R2 is hydrogen or methyl is provided.
摘要翻译： 根据式（I）的化合物：其中：A表示未被取代或任选被C 1-4烷基或芳基取代的C 1-4亚烷基; 或A与相邻的苯环形成5-8元稠合的脂族环; m为1至3的整数;每个R 1独立地选自卤素，C 1-4烷基，甲磺酰基，烷氧基，腈，二甲胺 ，亚甲二氧基和CF 3; 并且R 2是氢或甲基。
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公开(公告)号：US06191304B1
公开(公告)日：2001-02-20
申请号：US09551743
申请日：2000-04-18
IPC分类号： C07C6976
CPC分类号： C07D213/74 , C07C69/734 , C07C69/738 , C07D213/75
摘要： This invention relates to certain tricyclic compounds that are integrin receptor antagonists.
摘要翻译： 本发明涉及作为整联蛋白受体拮抗剂的某些三环化合物
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5.发明授权Substituted bis-acridines and related compounds as CCR5 receptor ligands, anti-inflammatory agents and anti-viral agents 失效取代的双吖啶和相关化合物作为CCR5受体配体，抗炎剂和抗病毒剂公开(公告)号：US06242459B1
公开(公告)日：2001-06-05
申请号：US09341171
申请日：1999-07-02
IPC分类号： A61K31473
CPC分类号： A61K31/00 , A61K31/473 , C07D219/12
摘要： This invention relates to substituted bis-acridines and related compounds which are ligands, in particular, antagonists of the CCR5 receptor. In addition, this invention relates to the treatment and prevention of disease states mediated by CCR5, including, but not limited to, asthma and atopic disorders, rheumatoid arthritis, atherosclerosis, psoriasis, auto immune diseases such as multiple sclerosis, and inflammatory bowel disease, all in mammals, by the use of substituted bis-acridines and related compounds which are CCR5 receptor antagonists. Also, since CCR5 is a co-receptor for the entry of HIV into cells, selective receptor ligands may be useful in the treatment of HIV infection.
摘要翻译： 本发明涉及取代的双吖啶和相关化合物，它们是CCR5受体的配体，特别是拮抗剂。 此外，本发明涉及治疗和预防由CCR5介导的疾病状态，包括但不限于哮喘和特应性疾病，类风湿性关节炎，动脉粥样硬化，牛皮癣，自身免疫疾病如多发性硬化和炎症性肠病， 所有这些都在哺乳动物中，通过使用取代的双吖啶和作为CCR5受体拮抗剂的相关化合物。 此外，由于CCR5是HIV进入细胞的共同受体，因此选择性受体配体可用于治疗HIV感染。
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公开(公告)号：US06221860B1
公开(公告)日：2001-04-24
申请号：US09423421
申请日：1999-11-08
IPC分类号： A01N4300
CPC分类号： A61K31/4427 , A61K31/397
摘要： This invention relates to methods for treating diseases or disorders mediated by lipid inflammatory mediators, arachidonic acid, its metabolites and/or platelet activating factor (PAF), which method comprises administration to a mammal in need thereof of an effective Coenzyme A independent transacylase (CoA-IT) inhibiting amount of a triphenylmethylazetidinone. This invention also relates to a method of treating or reducing inflammation in a mammal in need thereof, which comprises administering to said mammal an effective amount of a triphenylmethylazetidinone.
摘要翻译： 本发明涉及用于治疗由脂质炎症介质介导的疾病或病症的方法，花生四烯酸，其代谢物和/或血小板活化因子（PAF），该方法包括向有需要的哺乳动物施用有效的辅酶A独立转酰酶（CoA -IT）抑制量的三苯基甲基氮杂环丁酮。 本发明还涉及在有需要的哺乳动物中治疗或减轻炎症的方法，其包括向所述哺乳动物施用有效量的三苯基甲基氮杂环丁酮。
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公开(公告)号：US4352809A
公开(公告)日：1982-10-05
申请号：US299435
申请日：1981-09-04
IPC分类号： A61K31/47 , A61P25/24 , A61P25/26 , C07D217/04 , C07D217/06 , C07D498/04 , C07D513/04
CPC分类号： C07D513/04 , C07D217/04 , C07D217/06
摘要： Method of producing alpha.sub.2 antagonism by administering thiadiazolo- and oxadiazolotetrahydroisoquinoline compounds.
摘要翻译： 通过施用噻二唑并氧杂二唑四氢异喹啉化合物来产生α2拮抗作用的方法。
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8.发明授权7- and/or 8-Sulfur substituted 1,2,3,4-tetrahydroisoquinoline compounds 失效7-和/或8-硫取代的1,2,3,4-四氢异喹啉化合物
公开(公告)号：US4228170A
公开(公告)日：1980-10-14
申请号：US71203
申请日：1979-08-30
IPC分类号： C07D217/02 , C07D217/06 , A61K31/47
CPC分类号： C07D217/06 , C07D217/02
摘要： 1,2,3,4-Tetrahydroisoquinoline compounds having 7- and/or 8-sulfur substituents are inhibitors of phenylethanolamine N-methyltransferase.
摘要翻译： 具有7-和/或8-硫取代基的1,2,3,4-四氢异喹啉化合物是苯乙醇胺N-甲基转移酶的抑制剂。
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9.发明授权4- and 5-Substituted 2,3-dihydro-1H-isoindoles, pharmaceutical compositions and method of inhibiting phenylethanolamine N-methyltransferase 失效4-和5-取代的2,3-二氢-1H-异吲哚，药物组合物和抑制苯乙醇胺N-甲基转移酶的方法
公开(公告)号：US4218464A
公开(公告)日：1980-08-19
申请号：US17005
申请日：1979-03-02
IPC分类号： C07D209/44 , A61K31/40
CPC分类号： C07D209/44
摘要： Pharmaceutical compositions and methods of inhibiting phenylethanolamine N-methyltransferase using novel 2,3-dihydro-1H-isoindole compounds having 4- and 5-substituents.
摘要翻译： 使用具有4-和5-取代基的新型2,3-二氢-1H-异吲哚化合物抑制苯乙醇胺N-甲基转移酶的药物组合物和方法。
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公开(公告)号：US06476028B1
公开(公告)日：2002-11-05
申请号：US09529338
申请日：2000-08-08
申请人： William E. Bondinell , James Chan , Roderick A. Porter , Joseph W. Venslavsky , Steven Dabbs , David T. Davies
发明人： William E. Bondinell , James Chan , Roderick A. Porter , Joseph W. Venslavsky , Steven Dabbs , David T. Davies
IPC分类号： A61K3153
CPC分类号： C07D401/04 , A61K31/454 , C07D401/14
摘要： A method of treating a CCR5-mediated disease state in mammals which comprises administering to a mammal in need of such treatment, an effective amount of a compound of formula (I) or a pharmaceutically acceptable salt thereof.
摘要翻译： 一种治疗哺乳动物中CCR5介导的疾病状态的方法，其包括向需要这种治疗的哺乳动物施用有效量的式（I）化合物或其药学上可接受的盐。
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