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    • 1. 发明申请
    • 6-ARYL-IMIDAZ0[L, 2-A] PYRAZINE DERIVATIVES, METHOD OF MAKING, AND METHOD OF USE THEREOF
    • 6-ARYL-IMIDAZO [L,2-A]吡嗪衍生物,制备方法及其使用方法
    • WO2009102468A1
    • 2009-08-20
    • PCT/US2009/000919
    • 2009-02-12
    • CGI PHARMACEUTICALS, INC.MITCHELL, Scott A.CURRIE, Kevin S.BLOMGREN, Peter A.ARMISTEAD, David M.RAKER, Joseph
    • MITCHELL, Scott A.CURRIE, Kevin S.BLOMGREN, Peter A.ARMISTEAD, David M.RAKER, Joseph
    • C07D487/04A61K31/4985A61P37/00
    • C07D487/04
    • Certain chemical entities chosen from compounds represented by Formula I and pharmaceutically acceptable salts and mixtures thereof, are provided herein. Pharmaceutical compositions comprising at least one chemical entity and one or more pharmaceutically acceptable vehicle. Methods of treating patients suffering from certain diseases and disorders responsive to the inhibition of Syk activity, which comprises administering to such patients an amount of at least one chemical entity effective to reduce signs or symptoms of the disease or disorder are disclosed. These diseases include cancer (e.g., B -cell lymphoma and leukemia), autoimmune diseases, inflammatory diseases, acute inflammatory reactions, and allergic disorders. Methods of treatment include administering at least one chemical entity as a single active agent or administering at least one chemical entity in combination with one or more other therapeutic agents. Also provided are methods for determining the presence or absence of Syk kinase in a sample. Formula I
    • 在本文中提供了选自由式I表示的化合物的某些化学实体及其药学上可接受的盐及其混合物。 包含至少一种化学实体和一种或多种药学上可接受的载体的药物组合物。 公开了治疗患有对抑制Syk活性有反应的某些疾病和病症的患者的方法,所述方法包括向所述患者施用一定量的至少一种有效减少疾病或病症体征或症状的化学实​​体。 这些疾病包括癌症(例如,B细胞淋巴瘤和白血病),自身免疫疾病,炎性疾病,急性炎症反应和过敏性疾病。 治疗方法包括给予至少一种化学实体作为单一活性剂或与一种或多种其它治疗剂组合施用至少一种化学实体。 还提供了用于确定样品中Syk激酶的存在或不存在的方法。 一级方程式
    • 6. 发明申请
    • FUSED HETEROCYCLIC COMPOUNDS
    • 熔融杂环化合物
    • WO2012018909A1
    • 2012-02-09
    • PCT/US2011/046417
    • 2011-08-03
    • TAKEDA PHARMACEUTICAL COMPANY LIMITEDRAKER, JosephTANIGUCHI, TakahikoYOSHIKAWA, MasatoHASUI, TomoakiKUNITOMO, Jun
    • RAKER, JosephTANIGUCHI, TakahikoYOSHIKAWA, MasatoHASUI, TomoakiKUNITOMO, Jun
    • C07D471/04C07D471/14C07D519/00A61K31/437A61P25/18
    • C07D471/04C07D471/14C07D519/00
    • The present invention provides a compound which has the effect of PDE 10A inhibition, and which is useful as a medicament for preventing or treating schizophrenia or so on. A compound represented by the formula (1'): wherein, Ring A' represents an optionally substituted pyridine ring, an optionally substituted pyridazine ring, a pyrimidine ring, or 10 a pyrazine ring, R1' represents (1) wherein, R 1a' represents an optionally substituted phenyl group, or an optionally substituted 5- to 10-membered heterocyclic group, Ring B2 represents a bond, -S-, -0-, -CO-, an optionally substituted methylene group, or -NR a' - (R a' represents a hydrogen atom, or an optionally substituted C 1-6 alkyl group), and Ring B 1' represents an optionally further substituted 6- to 10- membered aromatic hydrocarbon ring, or an optionally further substituted 5- to 10-membered aromatic heterocyclic ring, or alternatively, L' and R 1a' may be taken together to form an optionally substituted bicyclic or tricyclic fused heterocyclic group, or (2), wherein, R 1b' represents an optionally substituted phenyl group, or an optionally substituted 5- to 10-membered heterocyclic group, Ring B 2' represents an optionally substituted benzene ring, an optionally substituted pyridine ring, an optionally substituted pyrimidine ring, an optionally substituted pyrazine ring, or an optionally substituted pyridazine ring, Ring D' represents an optionally further substituted 5- or 6- membered ring, R 2' represents a hydrogen atom, or a substituent, X' represents =N- or =CR b' - (R b' represents a hydrogen atom, or a substituent), _ _ _ _ _ represents that R b' and R 2' may form, taken together with the carbon atom and the nitrogen atom to which they are each adjacent, an optionally substituted 5- to 7-membered ring when.X' is =CR b' -, or a salt thereof.
    • 本发明提供了具有PDE 10A抑制作用的化合物,其可用作预防或治疗精神分裂症等的药物。 由式(1')表示的化合物:其中环A'表示任选取代的吡啶环,任选取代的哒嗪环,嘧啶环或吡嗪环,R1'表示(1)其中R1a'表示 任选取代的苯基或任选取代的5至10元杂环基,环B2表示键,-S - , - O-,-CO-,任选取代的亚甲基或-NR a' “表示氢原子或任选取代的C 1-6烷基),并且环B1'表示任选进一步取代的6-至10-元芳族烃环,或任选进一步取代的5至10元芳族杂环 ,或者可选地,L'和R 1a'可以一起形成任选取代的双环或三环稠合杂环基,或(2),其中,R 1b'表示任选取代的苯基,或任选取代的5-至10- 环B2'代表 任选取代的苯环,任选取代的吡啶环,任选取代的嘧啶环,任选取代的吡嗪环或任选取代的哒嗪环,环D'表示任选进一步取代的5-或6-元环,R 2' 表示氢原子或取代基,X'表示= N-或= CRb'-(Rb'表示氢原子或取代基),表示Rb'和R2'可以一起形成 与它们各自相邻的碳原子和氮原子,当X'= CRb'-时,任选取代的5-至7-元环,或其盐。