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    Thiadiazole compounds and methods of use thereof
    3.
    发明申请
    Thiadiazole compounds and methods of use thereof 审中-公开
    噻二唑化合物及其使用方法

    公开(公告)号：US20080125469A1

    公开(公告)日：2008-05-29

    申请号：US11810911

    申请日：2007-06-07

    申请人： Matthew G. Bursavich ,  Sabrina Lombardi ,  Adam M. Gilbert

    发明人： Matthew G. Bursavich ,  Sabrina Lombardi ,  Adam M. Gilbert

    IPC分类号： A61K31/433 ,  C07D285/14 ,  A61P35/00 ,  A61P19/02

    CPC分类号： C07D513/10

    摘要： The present invention relates to Thiadiazole Compounds; compositions comprising an effective dose of a Thiadiazole Compound; and methods treating or preventing a metalloproteinase-related disorder, such as, an arthritic disorder, osteoarthritis, cancer, rheumatoid arthritis, asthma, chronic obstructive pulmonary disease, atherosclerosis, age-related macular degeneration, myocardial infarction, a corneal ulceration, an ocular surface disease, hepatitis, an aortic aneurysm, tendonitis, a central nervous system disorder, abnormal wound healing, angiogenesis, restenosis, cirrhosis, multiple sclerosis, glomerulonephritis, graft versus host disease, diabetes, an inflammatory bowel disease, shock, invertebral disc degeneration, stroke, osteopenia or a periodontal disease or comprising administering an effective dose of a Thiadiazole Compound to a mammal in need thereof.

    摘要翻译： 本发明涉及噻二唑化合物; 包含有效剂量的噻二唑化合物的组合物; 以及治疗或预防金属蛋白酶相关疾病如关节炎疾病，骨关节炎，癌症，类风湿性关节炎，哮喘，慢性阻塞性肺病，动脉粥样硬化，年龄相关性黄斑变性，心肌梗塞，角膜溃疡，眼表面 疾病，肝炎，主动脉瘤，腱炎，中枢神经系统疾病，异常伤口愈合，血管生成，再狭窄，肝硬化，多发性硬化，肾小球性肾炎，移植物抗宿主病，糖尿病，炎性肠病，休克，椎间盘退变，中风 ，骨质减少或牙周病，或包括向有需要的哺乳动物施用有效剂量的噻二唑化合物。

    Substituted 1,3-benzodioxoles
    5.
    发明授权
    Substituted 1,3-benzodioxoles 失效
    取代的1,3-苯并二恶烷

    公开(公告)号：US5914339A

    公开(公告)日：1999-06-22

    申请号：US854199

    申请日：1997-05-09

    申请人： Fuk-Wah Sum ,  Adam M. Gilbert ,  George T. Grosu ,  Michael S. Malamas ,  Aranapakam M. Venkatesan ,  Gerardo D. Francisco

    发明人： Fuk-Wah Sum ,  Adam M. Gilbert ,  George T. Grosu ,  Michael S. Malamas ,  Aranapakam M. Venkatesan ,  Gerardo D. Francisco

    IPC分类号： C07D317/68 ,  C07D413/06 ,  A61K31/42 ,  A61K31/36 ,  C07D263/06 ,  C07D317/58

    CPC分类号： C07D413/06 ,  C07D317/68

    摘要： The present invention provides new compounds having anti-diabetic and/or antihyperglycemia and/or anti-obesity activity, as well as pharmaceutical compositions and methods of treatment utilizing the compounds and processes for making the compounds, the compounds having the formula (II): ##STR1## wherein: R.sub.1 and R.sub.6 are independently hydrogen, C.sub.1 to C.sub.6 alkyl, trifluoromethyl, cyano, C.sub.1 to C.sub.6 alkoxy, or halogen;R.sub.2 is hydrogen or C.sub.1 to C.sub.6 trialkylsilyl;R.sub.3 is hydrogen or C.sub.1 to C.sub.6 alkoxycarbonyl;or R.sub.2 and R.sub.3 are joined to form a ring: ##STR2## wherein R' is hydrogen, C.sub.1 to C.sub.6 alkyl, or aryl; R.sub.4 and R.sub.5 are independently hydrogen or C.sub.1 to C.sub.6 alkyl;R.sub.7 and R.sub.8 are independently OR.sub.9 or NR.sub.10 R.sub.11 ;R.sub.9 is hydrogen, C.sub.1 to C.sub.12 alkyl, C.sub.1 to C.sub.12 cycloalkyl, C.sub.1 to C.sub.12 silylalkyl, aryl, arylalkyl, alkoxyalkyl, heteroaryl, --CHR.sub.12 COOR.sub.13, --CHR.sub.12 C(O)R.sub.13, --CHR.sub.12 CONR.sub.1 R.sub.11, --CHR.sub.12 OCOOR.sub.13, or --CHR.sub.12 OC(O)R.sub.13, with the provision that R.sub.9 is not hydrogen in both R.sub.7 and R.sub.8 ;R.sub.10 and R.sub.11 are independently hydrogen, C.sub.1 to C.sub.12 alkyl, aralkyl, aryl, furanylalkyl, or alkoxycarbonylalkyl;R.sub.12 and R.sub.13 are independently hydrogen, C.sub.1 to C.sub.12 alkyl, aryl, or aralkyl; and the pharmaceutically acceptable salts thereof, the enantiomers thereof, the racemic mixtures thereof, and the diastereomeric mixtures thereof.

    摘要翻译： 本发明提供具有抗糖尿病和/或抗高血糖和/或抗肥胖活性的新化合物，以及利用该化合物的药物组合物和治疗方法以及制备该化合物的方法，具有式（II）的化合物： 其中：R 1和R 6独立地为氢，C 1至C 6烷基，三氟甲基，氰基，C 1至C 6烷氧基或卤素; R2是氢或C1-C6三烷基甲硅烷基; R3是氢或C1-C6烷氧基羰基; 或R2和R3连接形成环：其中R'是氢，C1-C6烷基或芳基; R4和R5独立地是氢或C1-C6烷基; R7和R8独立地是OR9或NR10R11; R 9是氢，C 1至C 12烷基，C 1至C 12环烷基，C 1至C 12甲硅烷基烷基，芳基，芳基烷基，烷氧基烷基，杂芳基，-CHR 12 COOR 13，-CHR 12 C（O）R 13，-CHR 12 CONR1R 11，-CHR 12 COOOR 13或-CHR 12 OC（O）R 13 ，其中R7和R8中的R9不是氢; R 10和R 11独立地为氢，C 1至C 12烷基，芳烷基，芳基，呋喃基烷基或烷氧基羰基烷基; R 12和R 13独立地为氢，C 1至C 12烷基，芳基或芳烷基; 及其药学上可接受的盐，其对映异构体，其外消旋混合物及其非对映体混合物。

    8-aza-bicyclo[3.2.1]octan-3-ol derivatives of 2,3-dihydro-1,4-benzodioxan as 5-HT1A antagonists
    8.
    发明授权
    8-aza-bicyclo[3.2.1]octan-3-ol derivatives of 2,3-dihydro-1,4-benzodioxan as 5-HT1A antagonists 失效
    2,3-二氢-1,4-苯并二恶烷的8-氮杂 - 双环[3.2.1]辛-3-醇衍生物，为5-HT 1A拮抗剂

    公开(公告)号：US06656951B2

    公开(公告)日：2003-12-02

    申请号：US10128057

    申请日：2002-04-23

    申请人： Adam M. Gilbert ,  Gary P. Stack

    发明人： Adam M. Gilbert ,  Gary P. Stack

    IPC分类号： A61K3146

    CPC分类号： C07D451/06

    摘要： Compounds of the formula: are useful for treating the cognitive deficits due to aging, stroke, head trauma, Alzheimer's disease or other neurodegenerative diseases, or schizophrenia and also treatment of disorders related to excessive serotonergic stimulation, such as anxiety, aggression and stress, and for the control of various physiological phenomena, such as appetite, thermoregulation, sleep and sexual behavior, which are known to be, at least in part, under serotonergic influence.

    摘要翻译： 下式的化合物可用于治疗由于老化，中风，头部创伤，阿尔茨海默氏病或​​其他神经变性疾病或精神分裂症引起的认知缺陷，以及治疗与过度5-羟色胺能刺激相关的疾病如焦虑，侵袭和压力，以及 用于控制各种生理现象，例如食欲，体温调节，睡眠和性行为，其已知至少部分地在5-羟色胺能影响下。

    Fluorinated N-arylmethylamino derivatives of cyclobutene-3,4-diones
    9.
    发明授权
    Fluorinated N-arylmethylamino derivatives of cyclobutene-3,4-diones 失效
    环丁烯-3,4-二酮的氟化N-芳基甲基氨基衍生物

    公开(公告)号：US5750574A

    公开(公告)日：1998-05-12

    申请号：US889163

    申请日：1997-07-07

    申请人： Adam M. Gilbert

    发明人： Adam M. Gilbert

    IPC分类号： C07C225/20 ,  C07C233/41 ,  C07C255/58 ,  A61K31/135 ,  A61K31/165 ,  C07C235/82

    CPC分类号： C07C255/58 ,  C07C225/20 ,  C07C233/41 ,  C07C2101/04

    摘要： A compound of the general formula (I) ##STR1## wherein R.sub.1 is straight chain alkyl, branched chain alkyl, cycloalkyl, hydroxyalkyl, fluoroalkyl or polyfluoroalkyl; R.sub.2 and R.sub.3 are, independently, hydrogen or an acyl substituent selected from the group consisting of formyl, alkanoyl, alkenoyl, alkylsulfonyl, aroyl, arylalkenoyl, arylsulfonyl, arylalkanoyl or arylalkylsulfonyl; A is a substituted phenyl group of the following formula: ##STR2## wherein R.sub.4 is F, perfluoroalkyl group of 1 to 10 carbon atoms or perfluoroalkoxy of 1 to 10 carbon atoms; or a pharmaceutically acceptable salt thereof relax smooth muscles.

    摘要翻译： 通式（I）的化合物其中R 1是直链烷基，支链烷基，环烷基，羟基烷基，氟烷基或多氟烷基; R2和R3独立地是氢或选自甲酰基，烷酰基，烯酰基，烷基磺酰基，芳酰基，芳基烯酰基，芳基磺酰基，芳基烷酰基或芳基烷基磺酰基的酰基取代基。 A是下式的取代苯基：其中R 4是F，1-10个碳原子的全氟烷基或1-10个碳原子的全氟烷氧基; 或其药学上可接受的盐使平滑肌松弛。

    Azabicyclylmethyl derivatives of 2,3-dihydro-1,4-dioxino[2,3-f]quinoline as 5-HT1A antagonists
    10.
    发明授权
    Azabicyclylmethyl derivatives of 2,3-dihydro-1,4-dioxino[2,3-f]quinoline as 5-HT1A antagonists 失效
    作为5-HT1A拮抗剂的2,3-二氢-1,4-二氧杂环己烯并[2,3-f]喹啉的二甲苯基甲基衍生物

    公开(公告)号：US06861427B2

    公开(公告)日：2005-03-01

    申请号：US10131355

    申请日：2002-04-24

    申请人： Gary P. Stack ,  Adam M. Gilbert ,  Megan Tran

    发明人： Gary P. Stack ,  Adam M. Gilbert ,  Megan Tran

    IPC分类号： A61P25/16 ,  A61P25/28 ,  C07D519/00 ,  A61K31/53 ,  A61K31/498 ,  A61K31/519 ,  C07D487/02

    CPC分类号： C07D519/00

    摘要： Compounds of the formula are useful for treating the cognitive deficits due to aging, stroke, head trauma, Alzheimer's disease or other neurodegenerative diseases, or schizophrenia, and are also useful for the treatment of disorders such as anxiety, aggression and stress, and for the control of various physiological phenomena, such eating disorders, disorders of thermoregulation, and sleep and sexual dysfunction.

    摘要翻译： 该化合物可用于治疗由于老化，中风，头部创伤，阿尔茨海默病或其他神经变性疾病或精神分裂症引起的认知缺陷，并且还可用于治疗诸如焦虑，侵袭和应激等疾病以及用于控制 的各种生理现象，这种进食障碍，体温调节障碍，以及睡眠和性功能障碍。