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    • 72. 发明申请
    • HETEROARYL-CONTAINING ISOFLAVONES AS AROMATASE INHIBITORS
    • 含杂原子的异黄酮作为芳香化酶抑制剂
    • WO2007001348A3
    • 2007-10-04
    • PCT/US2005030401
    • 2005-08-26
    • UNIV OHIO STATE RES FOUNDBRUEGGEMEIER ROBERT WKIM YOUNG-WOOHACKETT JOHN C
    • BRUEGGEMEIER ROBERT WKIM YOUNG-WOOHACKETT JOHN C
    • A01N43/00A61K31/424A61K31/497
    • C07D311/04C07D405/12
    • Compounds and methods useful for treating and prevention of cancer, particularly hormone-dependent breast cancer. Provided are compounds of formula I: wherein X is selected from O, N, S, SO, SO 2 , and S(CH 2 ) n , wherein n = 1 - 10; R 1 and R 2 may be the same or different and are selected from H, OH, OCH 3 , OCH 2 CH 3 , OCH 2 C 6 H 5 , NH 2 , NHCH 3 , N(CH 3 ) 2 , CH 3 , CH 2 CH 3 , CH 2 CH 2 CH 3 , CH(CH 3 ) 2 , C(CH 3 ) 3 , NO 2 , F, Cl, Br, CF 3 , SH, SCH 3 , SCH 2 CH 3 , OCOCH 3 , OCOC(CH 3 ) 3 , OCOCH 2 COOH, and CN; and R 3 is a nitrogen-containing heterocyclic ring. Also provided are method for treating or preventing cancer in a subject by administering a therapeutically effective amount of a heteroaryl-containing isoflavone, or a pharmaceutically acceptable salt or prodrug thereof, to a subject in need of treatment. Also provided is a method for the synthesis of 2-substituted isoflavones by first reacting deoxybenzoins with a phase transfer catalyst to provide a 2-(alkylthio)isoflavone; second deprotecting the 2-(alkylthio)isoflavone; and third applying selective debenzylation to form the final compound.
    • 用于治疗和预防癌症的化合物和方法,特别是激素依赖性乳腺癌。 提供了式I的化合物:其中X选自O,N,S,SO,SO 2和S(CH 2)n SUB >,其中n = 1-10; R 1和R 2可以相同或不同,并且选自H,OH,OCH 3,OCH 2, SUB <3>, 2 6 H 5 ,NH 2 , NHCH <3>,N(CH 3 2 ,CH 3 ,CH 2 CH 3 ,CH 2 CH 2 CH 3 ,CH(CH 3 ) C,CH,SUB,F,Cl,Br,CF 3, 3,SCH,SCH 3,SCH 2,SCH 3,SCH 3,SCH 3,SCH 3,SCH 3,SCH 3, 3),COCOCH 2,COOH和CN;其中, 并且R 3是含氮杂环。 还提供了通过向需要治疗的受试者施用治疗有效量的含杂芳基的异黄酮或其药学上可接受的盐或前药来治疗或预防受试者中的癌症的方法。 还提供了一种合成2-取代异黄酮的方法,首先使脱氧苯偶姻与相转移催化剂反应以提供2-(烷硫基)异黄酮; 第二步使2-(烷硫基)异黄酮脱保护; 第三次应用选择性去苄基化形成最终化合物。
    • 74. 发明申请
    • FEATURE ISOLATION FOR FREQUENCY-SHIFTING INTERFEROMETRY
    • 用于频率移位干涉的特征分离
    • WO2006036711A3
    • 2007-07-26
    • PCT/US2005033884
    • 2005-09-20
    • CORNING INCKULAWIEC ANDREW WTRONOLONE MARK JLEE CHRISTOPHER A
    • KULAWIEC ANDREW WTRONOLONE MARK JLEE CHRISTOPHER A
    • A01N43/00A61K31/397
    • G01B11/2441
    • Frequency-scanning interferometry is used for measuring test objects having multiple surface regions. The regions are distinguished and can be measured based on different measuring criteria. Interference data is gathered for the imageable portion of the test object from a plurality of interference patterns taken over substantially the same imageable portion at different measuring beam frequencies. The interference data is evaluated to determine topographical measures of associated points on the test object. The topographical measures are compared against a benchmark to distinguish between points on the test object that are within a first of the surface regions from points on a boundary separating the first surface region from one or more other surface regions of the imageable portion of the test object. The interference data of points within the first surface region are further evaluated to a higher accuracy.
    • 频率扫描干涉测量用于测量具有多个表面区域的测试对象。 区域是区别的,可以根据不同的测量标准进行测量。 从不同测量光束频率的基本上相同的可成像部分上拍摄的多个干涉图案收集测试对象的可成像部分的干扰数据。 对干扰数据进行评估,以确定测试对象上相关点的拓扑测量。 将地形测量与基准进行比较,以将分离第一表面区域与测试对象的可成像部分的一个或多个其他表面区域的边界上的点之间区分在第一表面区域内的测试对象上的点 。 进一步对第一表面区域内的点的干涉数据进行更高精度的评估。
    • 78. 发明申请
    • 2-PYRIDINYL[7-(SUBSTITUTED-PYRIDIN-4-YL) PYRAZOLO[1,5-A]PYRIMIDIN-3-YL]METHANONES
    • 2-吡啶基[7-(取代的吡啶-4-基)吡唑并[1,5-A]嘧啶-3-基]甲烷
    • WO2005084439A1
    • 2005-09-15
    • PCT/US2005/007238
    • 2005-03-02
    • DOV PHARMACEUTICAL, INC.SKOLNICK, Phil
    • SKOLNICK, Phil
    • A01N43/00
    • C07D487/04
    • The present invention provides novel 2-pyridinyl[7(pyridin-4-yl)pyrazolo[1,5­-a]pyrimidin-3-yl]methanones with at least one substituent on the 4-pyridinyl ring having the chemical structure of formula (I): The invention further provides compositions and methods employing the novel 2-pyridinyl[7-(pyridin-4-yl)pyrazolo[1,5-a]pyrimidin-3-yl]methanones of formula: (I) in to modulate GABA and GABA receptor physiology to elicit therapeutic responses in mammalian subjects to alleviate neurological or psychiatric disorders, including stroke, head trauma, epilepsy, pain, migraine, mood disorders, anxiety, post traumatic stress disorder, obsessive compulsive disorders, mania, bipolar disorders, schizophrenia, seizures, convulsions, tinnitus, neurodegenerative disorders including Alzheimer's disease, amyotrophic lateral sclerosis and Parkinson's disease, Huntington's chorea, depression, bipolar disorders, mania, trigeminal and other neuralgia, neuropathic pain, hypertension, cerebral ischemia, cardiac arrhythmia, myotonia, substance abuse, myoclonus, essential tremor, dyskinesia and other movement disorders, neonatal cerebral hemorrhage, and spasticity, as well as other psychiatric and neurological disorders mediated by GABA and/or GABA receptors.
    • 本发明提供了具有式(III)化学结构的4-吡啶基环上具有至少一个取代基的新的2-吡啶基[7(吡啶-4-基)吡唑并[1,5-a]嘧啶-3-基] I):本发明还提供了使用式(I)的新型2-吡啶基[7-(吡啶-4-基)吡唑并[1,5-a]嘧啶-3-基]甲酮调节的组合物和方法 GABA和GABA受体生理学,以在哺乳动物受试者中引发治疗反应以减轻神经或精神疾病,包括中风,头部创伤,癫痫,疼痛,偏头痛,情绪障碍,焦虑,创伤后应激障碍,强迫症,躁狂症,双相情感障碍, 精神分裂症,癫痫发作,抽搐,耳鸣,包括阿尔茨海默病,肌萎缩性侧索硬化和帕金森病,亨廷顿氏舞蹈病,抑郁症,双相情感障碍,躁狂症,三叉神经痛和其他神经痛的神经变性疾病,神经性疼痛,高血压,脑缺血, ardiac心律不齐,肌强直,药物滥用,肌阵挛,原发性震颤,运动障碍和其他运动障碍,新生儿脑出血和痉挛状态,以及由GABA和/或GABA受体介导的其他精神和神经障碍。