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1. 发明申请

US20080153870A1 COCAINE RECEPTOR BINDING LIGANDS 审中-公开
公开(公告)号：US20080153870A1
公开(公告)日：2008-06-26
申请号：US11863587
申请日：2007-09-28
申请人： Michael J. KUHAR , Frank I. CARROLL , John W. BOJA , Anita H. LEWIN , Philip ABRAHAM
发明人： Michael J. KUHAR , Frank I. CARROLL , John W. BOJA , Anita H. LEWIN , Philip ABRAHAM
IPC分类号： A61K31/439 , A61P25/00 , A61P25/24 , A61P25/32 , A61P25/34 , A61P15/00
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

US06358492B1 Dopamine transporter imaging ligand 失效
标题翻译：多巴胺转运蛋白成像配体
公开(公告)号：US06358492B1
公开(公告)日：2002-03-19
申请号：US08946007
申请日：1997-10-07
申请人： Michael J. Kuhar , Frank I. Carroll , John W. Boja , Anita H. Lewin , Philip Abraham
发明人： Michael J. Kuhar , Frank I. Carroll , John W. Boja , Anita H. Lewin , Philip Abraham
IPC分类号： C07D45102
CPC分类号： A61K51/0448 , C07D451/02
摘要： The 3&agr; isomer of RTI-55, RTI-352, is an effective in vivo binding ligand that reflects greater selectivity for the dopamine transporter than is observed with RTI-55. In addition, there is also a more rapid achievement of apparent equilibrium in the striatal-to-cerebellar ratio (compared to RTI-55) as the ratio peaks at about 30 min and is maintained for about 20 min thereafter. Such apparent equilibrium is useful in developing an approach to measuring the number of dopamine transporters present in tissues. Moreover, these results indicate that the utilization of 3&agr; isomers of a variety of 3&bgr;-(substituted phenyl)tropanes will result in greater selectivity for dopamine transporters and a more rapid of achievement of apparent equilibrium.
摘要翻译： RTI-55，RTI-352的3α异构体是一种有效的体内结合配体，其反映了对多巴胺转运蛋白的选择性高于用RTI-55观察到的选择性。另外，纹状体与小脑的比例（与RTI-55相比）的表观平衡也更快，因为在30分钟左右的比例达到峰值，此后保持约20分钟。这种表观平衡在开发测量组织中存在的多巴胺转运蛋白数量的方法中是有用的。此外，这些结果表明，使用各种3'-巯基（取代苯基）托烷的3α异构体将导致对多巴胺转运蛋白的更高选择性和更快速地达到表观平衡。

3. 发明授权

US5935953A Methods for controlling invertebrate pests using cocaine receptor binding ligands 失效
标题翻译：用可卡因受体结合配体控制无脊椎动物害虫的方法
公开(公告)号：US5935953A
公开(公告)日：1999-08-10
申请号：US823563
申请日：1997-03-25
申请人： Michael J. Kuhar , Frank I. Carroll , John W. Boja , Anita H. Lewin , Philip Abraham
发明人： Michael J. Kuhar , Frank I. Carroll , John W. Boja , Anita H. Lewin , Philip Abraham
IPC分类号： A61K31/46 , A61P25/00 , A61P25/24 , A61P25/30 , A61P43/00 , C07D451/02 , C07F7/22 , A61K31/535 , A61K31/44 , A01N43/42
CPC分类号： C07D451/02 , C07F7/2212
摘要： The invention relates to a method of controlling an invertebrate pest, comprising contacting the pest with a pest-controlling amount of an agent having substantial inhibitory activity toward a phenylethanolamine reuptake transporter as determined by radioactive octopamine reuptake inhibition assay is disclosed. Compositions comprising compounds capable of inhibiting the octopamine reuptake transporter include cocaine analogs. A process for inhibiting the feeding of an invertebrate pest comprising contacting said pest with a pest-controlling amount of an agent having substantial inhibitory activity toward a phenylethanolamine reuptake transporter as determined by radioactive octopamine reuptake inhibition assay, with the proviso that said agent is not cocaine. A process for delaying the maturation of a juvenile invertebrate by contacting it with an inhibitory amount of a phenylethanolamine reuptake transporter blocker is also disclosed. A radioactive phenylethanolamine reuptake inhibition assay for determining whether a given compound is an inhibitor of octopamine neuronal transport is also disclosed.
摘要翻译：本发明涉及一种控制无脊椎害虫的方法，其包括使害虫与害虫控制量的对苯基乙醇胺再摄取转运蛋白具有显着抑制活性的药剂接触，所述药物通过放射性的八聚胺再摄取抑制测定法测定。包含能够抑制章鱼胺再摄取转运蛋白的化合物的组合物包括可卡因类似物。一种抑制无脊椎害虫进食的方法，包括使所述有害生物与害虫控制量的苯基乙醇胺再吸收转运蛋白具有显着的抑制活性的药剂接触，所述方法是通过放射性章鱼胺再摄取抑制测定法确定的，条件是所述药剂不可卡因。还公开了一种通过使少年无脊椎动物与抑制量的苯乙醇胺再摄取转运蛋白阻断剂接触来延迟成熟的方法。还公开了用于确定给定化合物是否是章鱼胺神经元转运抑制剂的放射性苯乙醇胺再摄取抑制测定。

4. 发明授权

US5747503A Selective inhibitors of biogenic amine transporters 失效
公开(公告)号：US5747503A
公开(公告)日：1998-05-05
申请号：US746517
申请日：1996-11-12
申请人： Richard Rothman , Frank I. Carroll , Bruce Blough , Samuel W. Mascarella
发明人： Richard Rothman , Frank I. Carroll , Bruce Blough , Samuel W. Mascarella
IPC分类号： C07D487/18 , A61K31/40 , A61K31/403 , A61K31/435 , A61P25/00 , A61P25/24 , A61P25/26 , A61P43/00 , C07D209/58 , C07D209/70 , C07D451/00 , C07D471/08 , C07D221/22 , A61K31/46
CPC分类号： C07D471/08 , C07D209/70 , C07D451/00
摘要： The present invention provides a compound having the structure: ##STR1## wherein X, Y, and Z are independently H, Cl, Br, F, OCH.sub.3, I, or an alkyl group having 1 to 6 carbon atoms; and R is ##STR2## wherein n is 0 to 6, X' and Y' are independently H, Cl, F, CH.sub.3, C.sub.2 H.sub.5, C.sub.3 H.sub.7, C.sub.4 H.sub.9, OCH.sub.3, OH, CF.sub.3, OCF.sub.3, NO.sub.2, NH.sub.2, N(CH.sub.3).sub.2, NHCOCH.sub.3, NCS, NHCOCH.sub.2 Br, or N.sub.3, and (CH.sub.2).sub.n, if present, may be substituted with OH, OCH.sub.3, or an alkyl or alkenyl group having 1 to 3 carbon atoms. The present invention also provides a pharmaceutical composition comprising the compound above and a pharmaceutically acceptable carrier. The present invention further provides a method for treating a disease characterized by a dopamine deficiency which comprises administering to a subject in need of such treatment an amount of the pharmaceutical composition above effective to treat the disease.

5. 发明授权

US5298499A S-2-(substituted ethylamino)ethyl phosphorothioates 失效
标题翻译： S-2-（取代乙氨基）乙基硫代磷酸酯
公开(公告)号：US5298499A
公开(公告)日：1994-03-29
申请号：US726286
申请日：1991-07-05
申请人： Frank I. Carroll , Philip Abraham
发明人： Frank I. Carroll , Philip Abraham
IPC分类号： C07D277/36 , C07F9/165 , C07F9/6506 , C07F9/6539 , C07F9/6544 , A61K31/66 , C07C229/00 , C07C69/66 , C07D285/01
CPC分类号： C07F9/6544 , C07F9/1651 , C07F9/65067 , C07F9/6539
摘要： Substituted phosphorothioate derivatives and pharmaceutical compositions thereof as potential antiradiation agents are disclosed.
摘要翻译：公开了取代的硫代磷酸酯衍生物及其药物组合物作为潜在的抗辐射剂。

6. 发明授权

US4568757A Configurationally locked retinoids 失效
标题翻译：配置锁定的类维生素A
公开(公告)号：US4568757A
公开(公告)日：1986-02-04
申请号：US574741
申请日：1984-01-30
申请人： Frank I. Carroll , Anita H. Lewin
发明人： Frank I. Carroll , Anita H. Lewin
IPC分类号： C07C45/46 , C07C47/238 , C07C47/277 , C07C49/792 , C07C57/26 , C07C57/50 , C07C59/68 , C07C69/618 , C07C403/00 , C07D211/88 , C07D309/30 , C07D309/32 , C07D315/00 , C07C57/34
CPC分类号： C07D315/00 , C07C403/20 , C07C45/46 , C07C47/238 , C07C47/277 , C07C49/792 , C07C57/26 , C07C57/50 , C07C59/68 , C07D309/30 , C07B2200/09 , C07C2101/16 , Y10S514/859 , Y10S514/863
摘要： A group of retinoids having "vitamin A type" activity which have the structure ##STR1## wherein R3 is a trimethylcyclohexenylethylene, tetramethyltetrahydronaphthalene or methoxytrimethylphenylethylene group;R1 and R2 which are different are selected from --OH, --OR4 and --NHR, provided one of R1 and R2 is OH; R4 is alkyl of 1 to 20 carbons; and R is selected from the group consisting of hydrogen, alkyl of 1 to 4 carbons, hydroxyalkyl of 1 to 4 carbons, alkylhydroxyalkyl of 1 to 4 carbons, phenyl, hydroxyphenyl and carboxyphenyl, and R5 is a lactone or lactam of the structure ##STR2## and X is oxygen or NR where R is as above, and the pharmaceutically acceptable salts thereof.
摘要翻译：一组具有“维生素A型”活性的类维生素A具有结构 I. II。 III。 IV。其中R3是三甲基环己烯基乙烯，四甲基四氢萘或甲氧基三甲基苯基亚乙基; 不同的R 1和R 2选自-OH，-OR 4和-NHR，其中R 1和R 2之一是OH; R4是1〜20个碳的烷基; 并且R选自氢，1至4个碳的烷基，1至4个碳的羟烷基，1至4个碳的烷基羟基烷基，苯基，羟基苯基和羧基苯基，R5是结构为“IMAGE”的内酯或内酰胺（i）（ii）（iii）（iv），X是氧或NR，其中R如上所述，及其药学上可接受的盐。

7. 发明授权

US4436641A Refrigeration liquid with blue leak indicator and process of using same 失效
标题翻译：具有蓝色泄漏指示器的制冷液体及其使用方法
公开(公告)号：US4436641A
公开(公告)日：1984-03-13
申请号：US444884
申请日：1982-11-29
申请人： Dale E. Stelz , Frank I. Carroll , Wilson M. Whaley
发明人： Dale E. Stelz , Frank I. Carroll , Wilson M. Whaley
IPC分类号： C09K5/04
CPC分类号： C09K5/044
摘要： 1,4-Bis(2,4,6-trialkylanilino)anthraquinone wherein the alkyls on each anilino group are selected from the group consisting of methyl and ethyl and one of the three alkyls on each anilino group is different from the other two, e.g. 1,4-bis(2,6-diethyl-4-methylanilino)anthraquinone, is disclosed as an unusually effective blue dye suitable for use as a visual leak indicator in halocarbon refrigerants or in refrigeration liquids comprising a halocarbon refrigerant in admixture with a refrigeration oil.
摘要翻译： 1,4-二（2,4,6-三烷基苯胺基）蒽醌，其中每个苯胺基上的烷基选自甲基和乙基，每个苯胺基上的三个烷基中的一个不同于另外两个。公开了1,4-二（2,6-二乙基-4-甲基苯胺基）蒽醌作为非常有效的蓝色染料，其适用于卤代烃制冷剂或冷冻液体中的目视泄漏指示剂，该制冷液体包含与制冷剂混合的卤代烃制冷剂油。

8. 发明授权

US07291737B2 Cocaine receptor binding ligands 失效
标题翻译：可卡因受体结合配体
公开(公告)号：US07291737B2
公开(公告)日：2007-11-06
申请号：US10986352
申请日：2004-11-12
申请人： Michael J. Kuhar , Frank I. Carroll , John W. Boja , Anita H. Lewin , Philip Abraham
发明人： Michael J. Kuhar , Frank I. Carroll , John W. Boja , Anita H. Lewin , Philip Abraham
IPC分类号： 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。

9. 发明授权

US06706880B2 Cocaine receptor binding ligands 失效
标题翻译：可卡因受体结合配体
公开(公告)号：US06706880B2
公开(公告)日：2004-03-16
申请号：US09956159
申请日：2001-09-20
申请人： Frank I. Carroll , Michael J. Kuhar , John W. Boja , Anita H. Lewin , Philip Abraham
发明人： Frank I. Carroll , Michael J. Kuhar , John W. Boja , Anita H. Lewin , Philip Abraham
IPC分类号： C07D45102
CPC分类号： C07D451/02 , A61K51/0448 , A61K2123/00 , C07F7/2208
摘要： The invention relates to novel compounds which show high affinity for cocaine receptors in the brain, particularly dopamine and serotonin transporter sites. The compounds may be used as imaging or pharmaceutical agents, in the diagnosis and treatment of drug addiction, depression, anorexia and neurodegenerative diseases or in determining the doses of therapeutic agents that occupy significant numbers of receptors.
摘要翻译：本发明涉及对脑中可卡因受体表现出高亲和力的新化合物，特别是多巴胺和血清素转运蛋白位点。这些化合物可用作成像或药剂，用于诊断和治疗药物成瘾，抑郁症，厌食症和神经变性疾病，或用于确定占据大量受体的治疗剂的剂量。

10. 发明授权

US06531483B1 Cocaine receptor binding ligands 失效
公开(公告)号：US06531483B1
公开(公告)日：2003-03-11
申请号：US08706263
申请日：1996-09-04
申请人： Michael J. Kuhar , Frank I. Carroll , John W. Boja , Anita H. Lewin , Philip Abraham
发明人： Michael J. Kuhar , Frank I. Carroll , John W. Boja , Anita H. Lewin , Philip Abraham
IPC分类号： A61K3146
CPC分类号： C07D451/02 , A61K51/0448 , A61K2123/00 , C07F7/2208
摘要： The invention relates to novel compounds which show high affinity for cocaine receptors in the brain, particularly dopamine and serotonin transporter sites. The compounds may be used as imaging or pharmaceutical agents, in the diagnosis and treatment of drug addiction, depression, anorexia and neurodegenerative diseases.

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