Nematicidal trifluorobutenes
    1.
    发明授权
    Nematicidal trifluorobutenes 失效
    杀线虫三氟丁烯

    公开(公告)号:US06743814B2

    公开(公告)日:2004-06-01

    申请号:US10220775

    申请日:2002-09-05

    IPC分类号: A61K31421

    CPC分类号: A01N43/76 C07D263/46

    摘要: The present invention relates to novel trifluorobutenes of the formula (I) wherein R1 represents hydrogen; halogen; alkyl that is unsubstituted or substituted with halogen, hydroxy, alkoxy, alkylthio, alkylcarbonyloxy, haloalkylcarbonyloxy, or cyano; alkylsulfonyloxy; or phenyl that is unsubstituted or substituted with halogen, alkyl, haloalkyl, alkoxy, alkylthio, alkylsulfonyl, haloalkoxy, haloalkylthio, phenyl, phenoxy, cyano, or nitro; R2 represents hydrogen; halogen; alkyl that is unsubstituted or substituted with alkoxy or halogen; or alkoxycarbonyl; and n represents 0, 1 or 2, with the proviso that if R1 represents alkyl, then R2 does not represent halogen. The invention also relates to processes for their preparation and their use as nematicides.

    摘要翻译: 本发明涉及式(I)的新型三氟丁烯,其中R 1表示氢; 卤素; 未取代或被卤素,羟基,烷氧基,烷硫基,烷基羰基氧基,卤代烷基羰基氧基或氰基取代的烷基; 烷基磺酰氧基; 或未被取代或被卤素,烷基,卤代烷基,烷氧基,烷硫基,烷基磺酰基,卤代烷氧基,卤代烷硫基,苯基,苯氧基,氰基或硝基取代的苯基; R 2表示氢; 卤素; 未被取代或被烷氧基或卤素取代的烷基; 或烷氧基羰基; 和n表示0,1或2,条件是如果R 1表示烷基,则R 2不表示卤素。 本发明还涉及其制备方法及其作为杀线虫剂的用途。

    Heterocyclic inhibitors of p38
    3.
    发明授权
    Heterocyclic inhibitors of p38 有权
    p38的杂环抑制剂

    公开(公告)号:US06509363B2

    公开(公告)日:2003-01-21

    申请号:US09809854

    申请日:2001-03-16

    IPC分类号: A61K31421

    摘要: The present invention relates to inhibitors of p38, a mammalian protein kinase involved cell proliferation, cell death and response to extracellular stimuli. The invention also relates to methods for producing these inhibitors. The invention also provides pharmaceutical compositions comprising the inhibitors of the invention and methods of utilizing those compositions in the treatment and prevention of various disorders.

    摘要翻译: 本发明涉及p38的抑制剂,哺乳动物蛋白激酶涉及细胞增殖,细胞死亡和对细胞外刺激的反应。 本发明还涉及生产这些抑制剂的方法。 本发明还提供包含本发明抑制剂的药物组合物和利用这些组合物治疗和预防各种疾病的方法。

    PPAR delta activators
    6.
    发明授权
    PPAR delta activators 有权
    PPARδ激活剂

    公开(公告)号:US06787552B2

    公开(公告)日:2004-09-07

    申请号:US10344496

    申请日:2003-02-11

    IPC分类号: A61K31421

    摘要: Compounds of the general formula (I) or salts thereof and activators of PPAR&dgr; (peroxisome proliferator activated receptor &dgr;) containing the compounds or the salts as the active ingredient: wherein R1 and R2 each are hydrogen, C1-8 alkyl, an aryl or heterocyclic group which may be substituted, or the like; A is oxygen, sulfur, or the like; X1 and X2 are each a free valency, oxygen, S(O)p (wherein p is an integer of 0 to 2), C(═O), C(═O)NH, NHC(═O), CH═CH, or the like; Y is optionally substituted C1-8 alkylene; Z is oxygen or sulfur; R3 and R4 are each optionally substituted C1-8 alkyl; and R8 is hydrogen or C1-8 alkyl, with the proviso that when X1 is a free valency, X2 is not O or S(O)p, while when X1 is C(═O)NH, X2 is not a free valency.

    摘要翻译: 通式(I)的化合物或其盐和含有化合物或其盐作为活性成分的PPARdta(过氧化物酶体增殖物活化受体δ)的活化剂:其中R 1和R 2各自为氢,C 1-8 烷基,可被取代的芳基或杂环基等; A是氧,硫等; X 1和X 2各自为自由价,氧,S(O)p(其中p为0至2的整数),C(= O),C(= O)NH,NHC(= O),CH = CH等; Y是任选取代的C 1-8亚烷基; Z是氧或硫; R 3和R 4各自为任选取代的C 1-8烷基; 并且R 8是氢或C 1-8烷基,条件是当X 1是自由价时,X 2不是O或S(O)p,而当X 1是C(O) = O)NH,X 2不是自由价。

    Carbamic acid derivatives
    7.
    发明授权
    Carbamic acid derivatives 失效
    氨基甲酸衍生物

    公开(公告)号:US06596743B2

    公开(公告)日:2003-07-22

    申请号:US10008827

    申请日:2001-12-10

    IPC分类号: A61K31421

    摘要: The present invention is a compound of formula: wherein R1, R2, R2′, X, A1/A2 and B are as defined in the specification. These compounds may be used in the control or prevention of acute and/or chronic neurological disorders such as restricted brain function caused by bypass operations or transplants, poor blood supply to the brain, spinal cord injuries, head injuries, hypoxia caused by pregnancy, cardiac arrest, hypoglycaemia, Alzheimer's disease, Huntington's chorea, ALS, dementia caused by AIDS, eye injuries, retinopathy, cognitive disorders, memory deficits, schizophrenia, idiopathic parkinsonism or parkinsonism caused by medicaments as well as conditions which lead to glutamate deficiency functions, such as e.g. muscle spasms, convulsions, migraine, urinary incontinence, nicotine addiction, psychoses, opiate addiction, anxiety, vomiting, acute and chronic pain, dyskinesia and depression.

    摘要翻译: 本发明是下式的化合物:其中R1,R2,R2',X,A1 / A2和B如本说明书中所定义。这些化合物可用于控制或预防急性和/或慢性神经障碍,例如 作为由旁路手术或移植引起的限制性脑功能,脑供血不足,脊髓损伤,头部损伤,怀孕引起的缺氧,心脏骤停,低血糖,阿尔茨海默病,亨廷顿舞蹈症,ALS,艾滋病引起的痴呆,眼睛损伤 ,视网膜病变,认知障碍,记忆缺陷,精神分裂症,由药物引起的特发性帕金森综合症或帕金森综合征以及导致谷氨酸缺乏功能的病症,例如 肌肉痉挛,抽搐,偏头痛,尿失禁,尼古丁成瘾,精神病,鸦片成瘾,焦虑,呕吐,急性和慢性疼痛,运动障碍和抑郁症。