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1. 发明授权

US08795629B2 Radio-methyl vorozole and methods for making and using the same 有权
公开(公告)号：US08795629B2
公开(公告)日：2014-08-05
申请号：US12704114
申请日：2010-02-11
申请人： Sung Won Kim , Anat Biegon , Joanna S. Fowler
发明人： Sung Won Kim , Anat Biegon , Joanna S. Fowler
IPC分类号： A61K51/00 , A61M36/14
CPC分类号： C07D403/10 , A61K51/0453 , C07B2200/05 , C07D403/06 , G01N33/573 , G01N2333/90245 , G01N2800/52
摘要： Radiotracer vorozole compounds for in vivo and in vitro assaying, studying and imaging cytochrome P450 aromatase enzymes in humans, animals, and tissues and methods for making and using the same are provided. [N-radio-methyl] vorozole substantially separated from an N-3 radio-methyl isomer of vorozole is provided. Separation is accomplished through use of chromatography resins providing multiple mechanisms of selectivity.

2. 发明申请

US20100209344A1 Radio-methyl Vorozole and Methods for Making and Using the Same 有权
标题翻译：无线电甲基Vorozole及其使用方法
公开(公告)号：US20100209344A1
公开(公告)日：2010-08-19
申请号：US12704114
申请日：2010-02-11
申请人： Sung Won Kim , Anat Biegon , Joanna S. Fowler
发明人： Sung Won Kim , Anat Biegon , Joanna S. Fowler
IPC分类号： A61K51/04 , C07D403/10 , A61K49/10 , G01N33/573
CPC分类号： C07D403/10 , A61K51/0453 , C07B2200/05 , C07D403/06 , G01N33/573 , G01N2333/90245 , G01N2800/52
摘要： Radiotracer vorozole compounds for in vivo and in vitro assaying, studying and imaging cytochrome P450 aromatase enzymes in humans, animals, and tissues and methods for making and using the same are provided. [N-radio-methyl] vorozole substantially separated from an N-3 radio-methyl isomer of vorozole is provided. Separation is accomplished through use of chromatography resins providing multiple mechanisms of selectivity.
摘要翻译：提供用于体内和体外测定，研究和成像人，动物和组织中的细胞色素P450芳香酶的放射性星形化合物的方法，以及制备和使用它们的方法。提供了基本上与Vorozole的N-3放射性 - 甲基异构体分离的[N-放射性甲基]芴。通过使用提供多种选择性机制的色谱树脂实现分离。

3. 发明授权

US06387955B1 Enhanced anti-angiogenic activity of permanently charged derivatives of steroid hormones 失效
标题翻译：增强类固醇激素永久带电的衍生物的抗血管生成活性
公开(公告)号：US06387955B1
公开(公告)日：2002-05-14
申请号：US09562949
申请日：2000-05-03
申请人： Anat Biegon , Marcus E. Brewster
发明人： Anat Biegon , Marcus E. Brewster
IPC分类号： A61K3114
CPC分类号： A61K31/14
摘要： The present invention discloses the use of permanently charged steroid agonists or antagonists as potent anti-angiogenic compositions comprising as an active ingredient a compound of the general formulae I, II or III: wherein DRUG is any steroid agonist or antagonist, a mixed agonist-antagonist, or a partial agonist and the substituents are as defined in the specification.
摘要翻译：本发明公开了使用永久带电的类固醇激动剂或拮抗剂作为有效的抗血管生成组合物，其包含通式I，II或III的化合物作为活性成分：其中DRUG是任何类固醇激动剂或拮抗剂，混合激动剂 - 拮抗剂，或部分激动剂，并且取代基如说明书中所定义。

4. 发明授权

US5372813A Substituted 6-nitroquipazines, methods of preparation, and methods of use 失效
标题翻译：取代的6-硝基喹喔啉，制备方法和使用方法
公开(公告)号：US5372813A
公开(公告)日：1994-12-13
申请号：US994825
申请日：1992-12-22
申请人： Chester A. Mathis, Jr. , Anat Biegon , Scott E. Taylor , Joel D. Enas
发明人： Chester A. Mathis, Jr. , Anat Biegon , Scott E. Taylor , Joel D. Enas
IPC分类号： A61K51/04 , C07D215/38 , G01N33/567 , G01N33/60 , G01N33/94 , A61K49/00 , C07D401/00
CPC分类号： G01N33/9466 , A61K51/0459 , C07D215/38 , G01N33/567 , G01N33/60 , A61K2123/00
摘要： Disclosed is a substituted 6-nitroquipazine of the formula ##STR1## wherein R.sub.1, R.sub.2, R.sub.3, and R.sub.4 are each selected from the group consisting of H, Fl, CL, Br, I, CF.sub.3, CH.sub.2 CH.sub.2 F, CH.sub.3, CH.sub.2 CH.sub.3, and --CH(CH.sub.3).sub.2, and wherein one of R.sub.1, R.sub.2, R.sub.3, and R.sub.4 is other than H.Also disclosed is a method for measurement of serotonin uptake sites in a sample, in which a radioligand is incubated with a sample and then the radioactivity of the radioligand bound to the sample is determined, utilizing a radio labeled substituted 6-nitroquipazine as the radioligand. Also disclosed is a method of manufacture and method of use.
摘要翻译：公开了下式的取代的6-硝基奎匹嗪其中R 1，R 2，R 3和R 4各自选自H，Fl，CL，Br，I，CF 3，CH 2 CH 2 F，CH 3，CH 2 CH 3和 - CH（CH 3）2，并且其中R 1，R 2，R 3和R 4中的一个不是H.还公开了测量样品中的5-羟色胺摄取位点的方法，其中将放射性配体与样品一起温育，使用放射性标记的取代的6-硝基喹嗪作为放射性配体，测定与样品结合的放射性配体的放射性。还公开了一种制造方法和使用方法。

5. 发明申请

US20060167099A1 Use of compositions that increase glutamate receptor activity in treatment of brain injury 审中-公开
标题翻译：使用增加谷氨酸受体活性治疗脑损伤的组合物
公开(公告)号：US20060167099A1
公开(公告)日：2006-07-27
申请号：US10984556
申请日：2004-11-09
申请人： Anat Biegon , Esther Shohami
发明人： Anat Biegon , Esther Shohami
IPC分类号： A61K31/198 , A61K31/195
CPC分类号： A61K31/195 , A61K31/198
摘要： The present invention provides a method for treating a brain injury. This method comprises administering to a mammal afflicted with a brain injury a pharmaceutical composition therapeutically effective to increase glutamate receptor activity in the brain of said mammal. The pharmaceutical composition is to be administered after an acute postinjury phase of said affliction, a time when the level of NMDA receptor activity in the brain is below normal. The pharmaceutical composition may be administered subsequent to an initial treatment with an NMDA antagonist, the NMDA antagonist being administered during the acute postinjury phase of said affliction, a time when the level of NMDA receptor activity is above normal.
摘要翻译：本发明提供了治疗脑损伤的方法。该方法包括向患有脑损伤的哺乳动物施用治疗有效增加所述哺乳动物脑中谷氨酸受体活性的药物组合物。所述药物组合物应在所述痛苦的急性后期损伤期之后施用，这是脑中NMDA受体活性水平低于正常水平的时间。药物组合物可以在用NMDA拮抗剂进行初次治疗之后施用，NMDA拮抗剂在所述疼痛的急性后期期间施用，NMDA受体活性水平高于正常值的时间。

6. 发明授权

US6096740A Dexanabinol derivatives and their use as neuroprotective pharmaceutical compositions 失效
标题翻译：德西那诺衍生物及其作为神经保护药物组合物的用途
公开(公告)号：US6096740A
公开(公告)日：2000-08-01
申请号：US11814
申请日：1998-09-28
申请人： Raphael Mechoulam , Emil Pop , Mordechai Sokolovsky , Yoel Kloog , Anat Biegon
发明人： Raphael Mechoulam , Emil Pop , Mordechai Sokolovsky , Yoel Kloog , Anat Biegon
IPC分类号： C07D311/80 , C07D405/06 , A61K31/352 , A61K31/496 , C07D295/037 , C07D453/04
CPC分类号： C07D405/06 , C07D311/80
摘要： The present invention relates to pharmaceutical compositions for preventing or alleviating neurotoxicity. Said pharmaceutical compositions comprise as their active ingredient the stereospecific (+) enantiomers, having (3S,4S) configuration, of .DELTA..sup.6 -tetrahydrocannabinol (THC) type compounds of general formula (I), as defined hereinbelow. ##STR1##
摘要翻译： PCT No.PCT / US95 / 01470 Sec。 371日期：1998年9月28日 102（e）1998年9月28日PCT提交1995年2月6日PCT公布。出版物WO95 / 20958 日期：1995年8月10日本发明涉及用于预防或减轻神经毒性的药物组合物。所述药物组合物包含具有（3S，4S）构型的如下文所定义的通式（I）的DELTA 6-四氢大麻酚（THC）型化合物的立体有择（+）对映异构体作为其活性成分。

7. 发明授权

US6083990A Enhanced anti-angiogenic activity of permanently charged derivatives of steroid hormones 失效
标题翻译：增强类固醇激素永久带电的衍生物的抗血管生成活性
公开(公告)号：US6083990A
公开(公告)日：2000-07-04
申请号：US833074
申请日：1997-04-02
申请人： Anat Biegon , Marcus E. Brewster
发明人： Anat Biegon , Marcus E. Brewster
IPC分类号： A61K31/14 , A01N33/12
CPC分类号： A61K31/14
摘要： The present invention discloses the use of permanently charged steroid agonists or antagonists as potent anti-angiogenic compositions comprising as an active ingredient a compound of the general formulae I, II or III: ##STR1## wherein DRUG is any steroid agonist or antagonist, a mixed agonist-antagonist, or a partial agonist and the substituents are as defined in the specification.
摘要翻译：本发明公开了使用永久带电的类固醇激动剂或拮抗剂作为有效的抗血管生成组合物，其包含通式I，II或III的化合物作为活性成分：其中DRUG是任何类固醇激动剂或拮抗剂，混合激动剂 - 拮抗剂，或部分激动剂，并且取代基如说明书中所定义。

8. 发明授权

US5521215A NMDA-blocking pharmaceuticals 失效
标题翻译： NMDA阻断药物
公开(公告)号：US5521215A
公开(公告)日：1996-05-28
申请号：US192886
申请日：1994-02-07
申请人： Raphael Mechoulam , Mordechai Sokolovsky , Yoel Kloog , Anat Biegon
发明人： Raphael Mechoulam , Mordechai Sokolovsky , Yoel Kloog , Anat Biegon
IPC分类号： A61K31/35 , A61K31/352 , A61P25/00 , A61P25/08 , C07D311/80 , C07D405/04 , C07D405/06 , C07D405/12
CPC分类号： C07D405/06 , A61K31/35 , C07D311/80
摘要： Pharmaceutical compositions are described for preventing neurotoxicity, crising as active ingredient the stereospecific (+) enantiomer, having (3S,4S) configuration of .DELTA..sup.6 tetrahydrocannabinol type compounds. The compositions are particularly effective in alleviating and even preventing neurotoxicity due to acute injuries to the central nervous system, including mechanical trauma, compromised or reduced blood supply as may occur in cardiac arrest or stroke, or poisonings. They are also effective in the treatment of certain chronic degenerative diseases characterized by gradual neuronal loss.
摘要翻译：描述了用于预防神经毒性的药物组合物，其包含具有（3S，4S）构型的DELTA 6四氢大麻酚型化合物的立体特异性（+）对映异构体作为活性成分。组合物特别有效地减轻甚至预防由于中枢神经系统的急性损伤引起的神经毒性，包括机械创伤，心脏骤停或中风或中毒可能发生的受损或减少的血液供应。它们也有效治疗某些以逐渐神经元损失为特征的慢性退行性疾病。

9. 发明授权

US5434295A Neuroprotective pharmaceutical compositions of 4-phenylpinene derivatives and certain novel 4-phenylpinene compounds 失效
标题翻译： 4-苯基蒎烯衍生物和某些新型4-苯基辛烯化合物的神经保护药物组合物
公开(公告)号：US5434295A
公开(公告)日：1995-07-18
申请号：US192924
申请日：1994-02-07
申请人： Raphael Mechoulam , Aviva Breuer , Anat Biegon
发明人： Raphael Mechoulam , Aviva Breuer , Anat Biegon
IPC分类号： C07C69/753 , A61K31/22 , A61K31/05 , C07C39/17 , C07C69/01
CPC分类号： C07C69/753
摘要： The present invention provides certain novel 4-phenylpinene derivatives, and teaches how to use said novel derivatives and related compounds in pharmaceutical compositions that have utility in treating various pathological conditions associated with damage to the central nervous system. The active ingredient of the pharmaceutical compositions according to the present invention is a compound of the formula: ##STR1## wherein A - - - B designates an optional double bond, R.sub.1 designates a variety of organic moieties, G designates alkyl, halogen, or various oxy groups, and R.sub.3 designates various alkyl groups, ether groups, or combinations thereof.
摘要翻译：本发明提供了某些新的4-苯基蒎烯衍生物，并教导了如何在药物组合物中使用所述新型衍生物和相关化合物，其可用于治疗与中枢神经系统损伤相关的各种病理状况。根据本发明的药物组合物的活性成分是下式的化合物：其中A - - B表示任选的双键，R1表示多种有机部分，G表示烷基，卤素或各种氧基，R3表示各种烷基，醚基或其组合。

10. 发明授权

US5304367A In vivo brain imaging agent and method for diagnosis of psychiatric disorders 失效
标题翻译：体内脑成像剂和精神障碍诊断方法
公开(公告)号：US5304367A
公开(公告)日：1994-04-19
申请号：US614434
申请日：1990-11-16
申请人： Anat Biegon
发明人： Anat Biegon
IPC分类号： A61K51/04 , A61K51/12 , A61K49/02
CPC分类号： A61K51/1282 , A61K51/0446
摘要： A composition useful as an imaging agent comprises a beta adrenergic receptor antagonist compound, preferably iodopindolol, to which is covalently attached an iodine radioisotope such as .sup.123 I or .sup.124 I. This composition is used in a method for radioimaging beta adrenergic receptors in a tissue, preferably brain. In particular, the method is useful with the radioimaging technique of single photon emission computed tomography (SPECT) or positron emission tomography (PET). The above composition, as well as a kit comprising a set of one or more standard radiographic images of beta adrenergic receptors, are also useful in methods for (1) diagnosing an alteration in beta adrenergic receptors in a tissue, particularly brain; (2) diagnosing suicidal depression in a subject; and (3) detecting the therapeutic normalization of beta adrenergic receptor expression in a subject.
摘要翻译：可用作显像剂的组合物包含β-肾上腺素能受体拮抗剂化合物，优选碘吲哚洛尔，其共价连接碘放射性同位素如123I或124I。该组合物用于放射成像的组织，优选脑中的β肾上腺素能受体的方法。特别地，该方法对于单光子发射计算机断层摄影（SPECT）或正电子发射断层摄影（PET）的放射成像技术是有用的。上述组合物以及包含一组或多种β肾上腺素能受体的标准放射照相图像的试剂盒也可用于（1）诊断组织，特别是脑中β肾上腺素能受体的改变的方法中; （2）诊断受试者的自杀性抑郁症; 和（3）检测受试者中β肾上腺素能受体表达的治疗正常化。

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