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    Enhanced anti-angiogenic activity of permanently charged derivatives of steroid hormones
    3.
    发明授权
    Enhanced anti-angiogenic activity of permanently charged derivatives of steroid hormones 失效
    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

    Applicant: Anat Biegon ,  Marcus E. Brewster

    Inventor： Anat Biegon ,  Marcus E. Brewster

    IPC: A61K3114

    CPC classification number: A61K31/14

    Abstract: 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.

    Abstract translation: 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。

    Substituted 6-nitroquipazines, methods of preparation, and methods of use
    4.
    发明授权
    Substituted 6-nitroquipazines, methods of preparation, and methods of use 失效
    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

    Applicant: Chester A. Mathis, Jr. ,  Anat Biegon ,  Scott E. Taylor ,  Joel D. Enas

    Inventor： Chester A. Mathis, Jr. ,  Anat Biegon ,  Scott E. Taylor ,  Joel D. Enas

    IPC: A61K51/04 ,  C07D215/38 ,  G01N33/567 ,  G01N33/60 ,  G01N33/94 ,  A61K49/00 ,  C07D401/00

    CPC classification number: G01N33/9466 ,  A61K51/0459 ,  C07D215/38 ,  G01N33/567 ,  G01N33/60 ,  A61K2123/00

    Abstract: 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.

    Abstract translation: 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。

    Use of compositions that increase glutamate receptor activity in treatment of brain injury
    5.
    发明申请
    Use of compositions that increase glutamate receptor activity in treatment of brain injury 审中-公开
    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

    Applicant: Anat Biegon ,  Esther Shohami

    Inventor： Anat Biegon ,  Esther Shohami

    IPC: A61K31/198 ,  A61K31/195

    CPC classification number: A61K31/195 ,  A61K31/198

    Abstract: 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.

    Abstract translation: 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。

    Enhanced anti-angiogenic activity of permanently charged derivatives of steroid hormones
    7.
    发明授权
    Enhanced anti-angiogenic activity of permanently charged derivatives of steroid hormones 失效
    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

    Applicant: Anat Biegon ,  Marcus E. Brewster

    Inventor： Anat Biegon ,  Marcus E. Brewster

    IPC: A61K31/14 ,  A01N33/12

    CPC classification number: A61K31/14

    Abstract: 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.

    Abstract translation: 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。

    NMDA-blocking pharmaceuticals
    8.
    发明授权
    NMDA-blocking pharmaceuticals 失效
    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

    Applicant: Raphael Mechoulam ,  Mordechai Sokolovsky ,  Yoel Kloog ,  Anat Biegon

    Inventor： Raphael Mechoulam ,  Mordechai Sokolovsky ,  Yoel Kloog ,  Anat Biegon

    IPC: A61K31/35 ,  A61K31/352 ,  A61P25/00 ,  A61P25/08 ,  C07D311/80 ,  C07D405/04 ,  C07D405/06 ,  C07D405/12

    CPC classification number: C07D405/06 ,  A61K31/35 ,  C07D311/80

    Abstract: 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.

    Abstract translation: 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。

    Neuroprotective pharmaceutical compositions of 4-phenylpinene derivatives and certain novel 4-phenylpinene compounds
    9.
    发明授权
    Neuroprotective pharmaceutical compositions of 4-phenylpinene derivatives and certain novel 4-phenylpinene compounds 失效
    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

    Applicant: Raphael Mechoulam ,  Aviva Breuer ,  Anat Biegon

    Inventor： Raphael Mechoulam ,  Aviva Breuer ,  Anat Biegon

    IPC: C07C69/753 ,  A61K31/22 ,  A61K31/05 ,  C07C39/17 ,  C07C69/01

    CPC classification number: C07C69/753

    Abstract: 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.

    Abstract translation: 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。

    In vivo brain imaging agent and method for diagnosis of psychiatric disorders
    10.
    发明授权
    In vivo brain imaging agent and method for diagnosis of psychiatric disorders 失效
    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

    Applicant: Anat Biegon

    Inventor： Anat Biegon

    IPC: A61K51/04 ,  A61K51/12 ,  A61K49/02

    CPC classification number: A61K51/1282 ,  A61K51/0446

    Abstract: 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.

    Abstract translation: 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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