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1. 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。

2. 发明授权

US06660863B2 Process for synthesizing anhydroecgonine derivative 失效
标题翻译：合成脱氢嘌呤衍生物的方法
公开(公告)号：US06660863B2
公开(公告)日：2003-12-09
申请号：US10210168
申请日：2002-08-02
申请人： Kyoko Okano , Osamu Itoh
发明人： Kyoko Okano , Osamu Itoh
IPC分类号： C07D45102
CPC分类号： C07D451/02
摘要： The present invention relates to a process for synthesizing an anhydroecgonine derivative without using cocaine as a starting material, and a process for synthesizing a phenyltropane derivative by using said anhydroecgonine derivative as an intermediate for the synthesis. The present invention provides a process for synthesizing an anhydroecgonine derivative which comprises reacting a cycloheptatriene derivative represented by the formula (1): with a primary amine, a salt thereof or ammonia in the presence of a base to obtain an anhydroecgonine derivative, and a process for synthesizing a phenyltropane derivative by using said anhydroecgonine derivative. In the formula (1), n is an integer of 0 or 1; and R1 is a cyano group in the case of n being 0, and R1 is selected from an alkyl group and an aralkyl group in the case of n being 1.
摘要翻译：本发明涉及一种不使用可卡因作为起始原料合成脱氢gon根衍生物的方法，以及通过使用所述脱氢ec根衍生物作为合成中间体合成苯基丙烷衍生物的方法。本发明提供了一种合成脱氢嘌呤衍生物的方法，其包括使式（1）表示的环庚三烯衍生物与伯胺，其盐或氨在碱的存在下反应，得到脱氢靛宁衍生物，和方法用于通过使用所述脱氢ec根衍生物合成苯基丙烷衍生物。在式（1）中，n为0或1的整数; 在n为0的情况下，R 1为氰基，在n为1时，R 1选自烷基和芳烷基。

3. 发明授权

US06596868B2 Process for synthesizing anhydroecgonine derivative 失效
标题翻译：合成脱氢嘌呤衍生物的方法
公开(公告)号：US06596868B2
公开(公告)日：2003-07-22
申请号：US09773688
申请日：2001-02-02
申请人： Kyoko Okano , Osamu Itoh
发明人： Kyoko Okano , Osamu Itoh
IPC分类号： C07D45102
CPC分类号： C07D451/02
摘要： The present invention relates to a process for synthesizing an anhydroecgonine derivative without using cocaine as a starting material, and a process for synthesizing a phenyltropane derivative by using said anhydroecgonine derivative as an intermediate for the synthesis. The present invention provides a process for synthesizing an anhydroecgonine derivative which comprises reacting a cycloheptatriene derivative represented by the formula (1): with a primary amine, a salt thereof or ammonia in the presence of a base to obtain an anhydroecgonine derivative, and a process for synthesizing a phenyltropane derivative by using said anhydroecgonine derivative. In the formula (1), n is an integer of 0 or 1; and R1 is a cyano group in the case of n being 0, and R1 is selected from an alkyl group and an aralkyl group in the case of n being 1.
摘要翻译：本发明涉及一种不使用可卡因作为起始原料合成脱氢gon根衍生物的方法，以及通过使用所述脱氢ec根衍生物作为合成中间体合成苯基丙烷衍生物的方法。本发明提供了一种合成脱氢嘌呤衍生物的方法，其包括使式（1）表示的环庚三烯衍生物与伯胺，其盐或氨在碱的存在下反应，得到脱氢靛宁衍生物，和方法用于通过使用所述脱氢ec根衍生物合成苯基丙烷衍生物。在式（1）中，n为0或1的整数; 在n为0的情况下，R 1为氰基，n为1时，R 1选自烷基和芳烷基。

4. 发明授权

US06316624B1 Process for the preparation of substituted 8-azabicyclo[3,2,1]octanes 失效
标题翻译：制备取代的8-氮杂双环[3,2,1]辛烷的方法
公开(公告)号：US06316624B1
公开(公告)日：2001-11-13
申请号：US09555429
申请日：2000-05-30
申请人： Martin Charles Bowden , Stephen Martin Brown
发明人： Martin Charles Bowden , Stephen Martin Brown
IPC分类号： C07D45102
CPC分类号： C07D451/02 , C07D491/10
摘要： A process for preparing a compound of formula (IV) wherein R1 is C1-4 alkyl, C1-4 haloalkyl, benzyl, C3-6 alkenyl or C3-6 alkyny, (provided that the &agr;-carbon atom of R1 is neither unsaturated nor substituted with halogen), which comprises reacting a compound of formula (III) with a source of hydroxylamine in the presence of an acid. Compounds of formula (IV) are agrochemical intermediates.
摘要翻译：制备式（IV）化合物的方法，其中R 1为C 1-4烷基，C 1-4卤代烷基，苄基，C 3-6烯基或C 3-6炔基（条件是R 1的α-碳原子既不饱和也不是被卤素取代），其包括在酸的存在下使式（III）化合物与羟胺源反应。式（Ⅳ）化合物是农药中间体。

5. 发明授权

US06486323B1 Process for producing optically active tropinonemonocarboxylic acid derivative 有权
标题翻译：光学活性托品酮一羧酸衍生物的制备方法
公开(公告)号：US06486323B1
公开(公告)日：2002-11-26
申请号：US09806592
申请日：2001-03-30
申请人： Manabu Node , Soichi Nakamura , Daisaku Nakamura
发明人： Manabu Node , Soichi Nakamura , Daisaku Nakamura
IPC分类号： C07D45102
CPC分类号： C12P17/10 , C12P41/00 , C12P41/005
摘要： An optically active tropinonemonocarboxylic acid ester derivative useful as an intermediate for synthesis of optically active tropane derivatives was obtained by reacting succindialdehyde with an organic amine and acetonedicarboxylic acid ester to obtain a tropinonedicarboxylic acid ester derivative, and then subjecting this derivative to enzyme-catalyzed asymmetric dealkoxy-carbonylation. Since anhydroecgonine methyl ester derived from the optically active tropinone-monocarboxylic acid ester derivative by reduction and dehydration had the same direction of optical rotation as in the case of anhydroecgonine methyl ester obtained from natural cocaine, it was proved that the obtained optically active tropinonemonocarboxylic acid ester derivative had the same absolute configuration as that of natural cocaine. The yield of the optically active tropinonemonocarboxylic acid ester derivative from the asymmetric dealkoxycarbonylation was 30 to 50 mol %, and its optical purity was 70 to 97% ee. In addition, it was found that a crystalline optically active anhydroecgonine carboxylic acid ester derivative can be obtained by reducing and then dehydrating the optically active tropinonemonocarboxylic acid ester derivative and that its optical purity can easily be increased by recrystallization.
摘要翻译：通过使琥珀醛与有机胺和丙酮二羧酸酯反应得到托品酮二羧酸酯衍生物，然后将该衍生物进行酶催化的不对称脱烷基，得到用作合成光学活性托烷衍生物的中间体的光学活性托品酮单羧酸酯衍生物羰基化。由于通过还原和脱水衍生自光学活性的托品酮 - 单羧酸酯衍生物的脱氢异君子酸甲酯具有与从天然可卡因得到的脱氢山梨醇甲酯的情况相同的旋光方向，所以证明得到的光学活性托品酮单羧酸酯衍生物具有与天然可卡因相同的绝对构型。来自不对称脱烷基羰基化反应的光学活性托品酮二羧酸酯衍生物的收率为30〜50摩尔％，光学纯度为70〜97％ee。此外，发现通过使光学活性托品酮一羧酸酯衍生物还原然后使其脱水，可以得到结晶光学活性的脱氢gon根化羧酸酯衍生物，并且可以通过重结晶容易地提高其光学纯度。

6. 发明授权

US06329520B1 Cocaine receptor binding ligands 失效
标题翻译：可卡因受体结合配体
公开(公告)号：US06329520B1
公开(公告)日：2001-12-11
申请号：US09083043
申请日：1998-05-22
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。

7. 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。

8. 发明授权

US06552036B2 3-(Diarylmethylene)-8-azabicyclo[3.2.1]octane derivatives 有权
标题翻译： 3-（二芳基亚甲基）-8-氮杂双环[3.2.1]辛烷衍生物
公开(公告)号：US06552036B2
公开(公告)日：2003-04-22
申请号：US09791246
申请日：2001-02-22
申请人： Robert E. Boyd , John R. Carson , Steven J. Coats , Lou Anne Neilson , Philip M Pitis , Wu-Nan Wu
发明人： Robert E. Boyd , John R. Carson , Steven J. Coats , Lou Anne Neilson , Philip M Pitis , Wu-Nan Wu
IPC分类号： C07D45102
CPC分类号： C07D451/02 , A61K31/439
摘要： This invention is directed to 3-(diarylmethylene)-8-azabicyclo[3.2.1]octane derivatives useful as &dgr;-opioid or &mgr;-opioid receptor modulators. Depending on their agonist or antagonist effect, the compounds are useful analgesics, immunosuppressants, antiinflammatory agents, agents for the treatment of neurological and psychiatric conditions, medicaments for drug and alcohol abuse, agents for treating gastritis and diarrhea, cardiovascular agents and agents for the treatment of respiratory diseases.
摘要翻译：本发明涉及可用作δ-阿片样物质或μ-阿片受体调节剂的3-（二芳基亚甲基）-8-氮杂双环[3.2.1]辛烷衍生物。根据其激动剂或拮抗剂的作用，化合物是有用的止痛剂，免疫抑制剂，抗炎剂，用于治疗神经和精神病症的药剂，用于药物和酒精滥用的药物，用于治疗胃炎和腹泻的药剂，用于治疗的心血管药剂和药剂的呼吸系统疾病。

9. 发明授权

US06323343B1 Process for the preparation of 8-azabicyclo(3.2.1)octane derivatives 失效
标题翻译：制备8-氮杂双环（3.2.1）辛烷衍生物的方法
公开(公告)号：US06323343B1
公开(公告)日：2001-11-27
申请号：US09555463
申请日：2000-05-30
申请人： Martin Charles Bowden , Stephen Martin Brown , Douglas John Smith , Trevor Robert Perrior
发明人： Martin Charles Bowden , Stephen Martin Brown , Douglas John Smith , Trevor Robert Perrior
IPC分类号： C07D45102
CPC分类号： C07D451/02
摘要： A process for preparing a compound of formula (IV), wherein R1 is C1-4alkyl, CH2(C1-3haloalkyl), benzyl, CH2(C2-5akenyl or CH2(C2-5alkynyl), which comprises reducing a compound of formula (III). Compounds of formula (IV) are agrochemical intermediates.
摘要翻译：一种制备式（IV）化合物的方法，其中R 1是C 1-4烷基，CH 2（C 1-3卤代烷基），苄基，CH 2（C 2-烯基或CH 2（C 2-5炔基）），其包括将式）式（Ⅳ）化合物是农药中间体。

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