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1. 发明申请

US20050197360A1 Cocaine receptor binding ligands 失效
标题翻译：可卡因受体结合配体
公开(公告)号：US20050197360A1
公开(公告)日：2005-09-08
申请号：US10986352
申请日：2004-11-12
申请人： Michael Kuhar , Frank Carroll , John Boja , Anita Lewin , Philip Abraham
发明人： Michael Kuhar , Frank Carroll , John Boja , Anita Lewin , Philip Abraham
IPC分类号： A61K31/46 , C07D451/02
CPC分类号： C07D451/02 , A61K31/439
摘要： A class of binding ligands for cocaine receptors and other receptors in the brain. Specifically, a novel family of compounds shows high binding specificity and activity, and, in a radiolabeled form, can be used to bind to these receptors, for biochemical assays and imaging techniques. Such imaging is useful for determining effective doses of new drug candidates in human populations. In addition, the high specificity, slow onset and long duration of the action of these compounds at the receptors makes them particularly well suited for therapeutic uses, for example as substitute medication for psychostimulant abuse. Some of these compounds may be useful in treating Parkinson's Disease or depression, by virtue of their inhibitory properties at monoamine transporters.
摘要翻译：一类可卡因受体和脑中其他受体的结合配体。具体来说，新型化合物家族显示出高结合特异性和活性，并且以放射性标记的形式可用于结合这些受体，用于生物化学测定和成像技术。这种成像可用于确定人群中新的候选药物的有效剂量。此外，这些化合物在受体的高度特异性，缓慢发作和长时间的作用使得它们特别适用于治疗用途，例如作为精神兴奋剂滥用的替代药物。这些化合物中的一些可能由于其在单胺转运蛋白上的抑制性质而可用于治疗帕金森病或抑郁症。

2. 发明授权

US6017957A Partial agonists of the strychnine insensitive glycine modulatory site of the N-methyl-D-aspartate receptor complex as neuropsychopharmacological agents 失效
标题翻译： N-甲基-D-天冬氨酸受体复合物的士的宁不敏感的甘氨酸调节位点的部分激动剂作为神经精神药理学试剂
公开(公告)号：US6017957A
公开(公告)日：2000-01-25
申请号：US390745
申请日：1989-08-08
申请人： Phil Skolnick , Anita Lewin , Juan-Carlos Marvizon , James Monn , Kenner Rice
发明人： Phil Skolnick , Anita Lewin , Juan-Carlos Marvizon , James Monn , Kenner Rice
IPC分类号： A61K31/195 , A61K31/215 , A61K45/00 , A61P25/00 , A61P25/18 , A61P25/20 , A61P25/28
CPC分类号： A61K31/195 , A61K31/215
摘要： A method is disclosed for the treatment of neuropsychopharmacological disorders which are associated with or result from excessive activation of the N-methyl-D-aspartate receptor complex, which method comprises administering an effective neuropsychopharmacological disorder-treating amount of a compound possessing partial agonist properties for the strychnine insensitive glycine modulatory sites of N-methyl-D-aspartate receptors. Exemplary of partial agonists which are useful in the method of the invention are 1-aminocyclopropanecarboxylic acid, and associated derivates thereof. Novel injectable pharmaceutical compositions are also disclosed.
摘要翻译：公开了用于治疗与N-甲基-D-天冬氨酸受体复合物的过量活化相关或由其引起的神经精神药理学障碍的方法，该方法包括给予有效的神经精神药理学障碍治疗量的具有部分激动剂性质的化合物 N-甲基-D-天冬氨酸受体的士的宁不敏感的甘氨酸调节位点。可用于本发明方法的部分激动剂的实例是1-氨基环丙烷羧酸及其相关衍生物。还公开了新的可注射药物组合物。

3. 发明授权

US5436369A Alicyclic phospholipase A.sub.2 inhibitors 失效
标题翻译：脂环磷脂酶A2抑制剂
公开(公告)号：US5436369A
公开(公告)日：1995-07-25
申请号：US200798
申请日：1994-02-23
申请人： Joanne J. Bronson , Katharine M. Greene , Muzammil M. Mansuri , Stanley V. D'Andrea , F. Ivy Carroll , Anita Lewin
发明人： Joanne J. Bronson , Katharine M. Greene , Muzammil M. Mansuri , Stanley V. D'Andrea , F. Ivy Carroll , Anita Lewin
IPC分类号： C07C69/612 , A61K31/19 , A61P29/00 , C07C63/66 , C07C67/30 , C07C69/00 , C07C69/618 , C07C69/65 , C07C69/734 , C07C69/76 , C07C69/94 , C07C63/64
CPC分类号： C07C63/66 , C07C69/618 , C07C69/65 , C07C69/734 , C07C69/76 , C07C69/94 , C07C2103/74
摘要： Certain novel alicyclic compounds are effective phospholipase A.sub.2 (PLA.sub.2) inhibitors.
摘要翻译：某些新型脂环化合物是有效的磷脂酶A2（PLA2）抑制剂。

4. 发明授权

US5141959A Isoprenoid phospholipase A2 inhibitors and preparations comprising same 失效
标题翻译：异噻唑类磷脂酶A2抑制剂和包含其的制剂
公开(公告)号：US5141959A
公开(公告)日：1992-08-25
申请号：US586159
申请日：1990-09-21
申请人： F. Ivy Carroll , Anita Lewin , Kenneth Tramposch , Stephen A. Steiner
发明人： F. Ivy Carroll , Anita Lewin , Kenneth Tramposch , Stephen A. Steiner
IPC分类号： A61K31/19 , A61K31/00 , A61K31/20 , A61K31/202 , A61K31/203 , A61K31/23 , A61K31/235 , A61P17/00 , A61P29/00 , C07C63/64 , C07C63/66 , C07C69/78 , C07C403/20 , C12N9/99
CPC分类号： C07C63/64 , C07C403/20 , C07B2200/09 , C07C2101/16
摘要： Compounds of the formula ##STR1## wherein R.sub.1 is CH.dbd.CY--C(CH.sub.3).dbd.CHX wherein X and Y are different and each is of the formula ##STR2## wherein R' and R" independently are H or alkyl of C.sub.1-6 and R.sub.1 includes all possible geometric isomers are demonstrated effective in treating inflammation, both topically and internally. The mechanism appears to be the inhibition of phospholipase A.sub.2 enzymes.

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