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    Fused heterocyclic compounds
    2.
    发明授权
    Fused heterocyclic compounds 有权

    公开(公告)号：US09029536B2

    公开(公告)日：2015-05-12

    申请号：US13814073

    申请日：2011-08-03

    申请人： Joseph Raker ,  Takahiko Taniguchi ,  Masato Yoshikawa ,  Tomoaki Hasui ,  Jun Kunitomo

    发明人： Joseph Raker ,  Takahiko Taniguchi ,  Masato Yoshikawa ,  Tomoaki Hasui ,  Jun Kunitomo

    IPC分类号： C07D471/04 ,  C07D471/14 ,  C07D519/00

    CPC分类号： C07D471/04 ,  C07D471/14 ,  C07D519/00

    摘要： 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, R1a′ 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 —NRa′— (Ra′ represents a hydrogen atom, or an optionally substituted C1-6 alkyl group), and Ring B1′ 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 R1a′ may be taken together to form an optionally substituted bicyclic or tricyclic fused heterocyclic group, or (2), wherein, R1b′ represents an optionally substituted phenyl group, or an optionally substituted 5- to 10-membered heterocyclic group, Ring B2′ 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, R2′ represents a hydrogen atom, or a substituent, X′ represents ═N— or ═CRb′—(Rb′ represents a hydrogen atom, or a substituent), - - - - - represents that Rb′ and R2′ 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 ═CRb′, or a salt thereof.

    Imidazopyrazine SYK inhibitors
    3.
    发明授权
    Imidazopyrazine SYK inhibitors 有权
    咪唑吡嗪SYK抑制剂

    公开(公告)号：US08697699B2

    公开(公告)日：2014-04-15

    申请号：US13343624

    申请日：2012-01-04

    申请人： Scott A. Mitchell ,  Peter A. Blomgren ,  Joseph Raker

    发明人： Scott A. Mitchell ,  Peter A. Blomgren ,  Joseph Raker

    IPC分类号： A61K31/495

    CPC分类号： C07D487/04

    摘要： Imidazopyrazines of 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 are also provided. 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.

    摘要翻译： 本文提供了式I的咪唑并嗪及其药学上可接受的盐和混合物。 还提供了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。

    Chemical sensors and method of use
    6.
    发明授权
    Chemical sensors and method of use 失效
    化学传感器及使用方法

    公开(公告)号：US06586256B1

    公开(公告)日：2003-07-01

    申请号：US09562202

    申请日：2000-05-02

    申请人： Timothy E. Glass ,  Joseph Raker ,  Ricardo Moran

    发明人： Timothy E. Glass ,  Joseph Raker ,  Ricardo Moran

    IPC分类号： G01N2164

    CPC分类号： G01N21/6428 ,  G01N2021/7786

    摘要： Chemical sensor compositions and methods for quantifying analytes are described. The chemical sensors include analyte-binding moieties and reporter moieties covalently attached to a framework including two trityl groups connected by a linear spacer such as ethyne or butadiyne. The sensors chelate an analyte across the acetylene axis of the molecule to stabilize the molecule in an eclipsed rotamer conformation. This conformation causes the sensors to emit a measurable signal. Also disclosed are methods of making the chemical sensors, methods of using the chemical sensors, and kits for quantifying analytes using the chemical

    摘要翻译： 描述了用于定量分析物的化学传感器组合物和方法。 化学传感器包括共价连接到框架上的分析物结合部分和报道部分，其包括通过线性间隔物例如乙炔或丁二炔连接的两个三苯甲基。 传感器通过分子的乙炔轴螯合分析物，以将分子稳定在黯淡的旋转异构体构象中。 这种构造使得传感器发出可测量的信号。 还公开了制备化学传感器的方法，使用化学传感器的方法以及使用该化学品定量分析物的试剂盒

    FUSED HETEROCYCLIC COMPOUNDS
    7.
    发明申请
    FUSED HETEROCYCLIC COMPOUNDS 有权
    熔融杂环化合物

    公开(公告)号：US20130172292A1

    公开(公告)日：2013-07-04

    申请号：US13814073

    申请日：2011-08-03

    申请人： Joseph Raker ,  Takahiko Taniguchi ,  Masato Yoshikawa ,  Tomoaki Hasui ,  Jun Kunitomo

    发明人： Joseph Raker ,  Takahiko Taniguchi ,  Masato Yoshikawa ,  Tomoaki Hasui ,  Jun Kunitomo

    IPC分类号： C07D471/04 ,  C07D471/14 ,  C07D519/00

    CPC分类号： C07D471/04 ,  C07D471/14 ,  C07D519/00

    摘要： 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, R1a′ 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 —NRa′-(Ra′ represents a hydrogen atom, or an optionally substituted C1-6 alkyl group), and Ring B1′ 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 R1a′ may be taken together to form an optionally substituted bicyclic or tricyclic fused heterocyclic group, or (2), wherein, R1b′ represents an optionally substituted phenyl group, or an optionally substituted 5- to 10-membered heterocyclic group, Ring B2′ 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, R2′ represents a hydrogen atom, or a substituent, X′ represents ═N— or ═CRb′—(Rb′ represents a hydrogen atom, or a substituent), - - - - - represents that Rb′ and R2′ 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 ═CRb′, or a salt thereof.

    摘要翻译： 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' - （R 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'表示 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'或其盐时，任选取代的5-至7-元环。

    CERTAIN SUBSTITUTED AMIDES, METHOD OF MAKING, AND METHOD OF USE THEREOF
    9.
    发明申请
    CERTAIN SUBSTITUTED AMIDES, METHOD OF MAKING, AND METHOD OF USE THEREOF 审中-公开
    某些替代的制剂，制备方法及其使用方法

    公开(公告)号：US20090221612A1

    公开(公告)日：2009-09-03

    申请号：US12370103

    申请日：2009-02-12

    申请人： Scott A. Mitchell ,  Kevin S. Currie ,  Peter A. Blomgren ,  David M. Armistead ,  Joseph Raker

    发明人： Scott A. Mitchell ,  Kevin S. Currie ,  Peter A. Blomgren ,  David M. Armistead ,  Joseph Raker

    IPC分类号： A61K31/519 ,  C07D487/04 ,  A61P35/00

    CPC分类号： C07D487/04

    摘要： 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.

    摘要翻译： 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。

    Rifamycin analogs and uses thereof
    10.
    发明授权
    Rifamycin analogs and uses thereof 失效
    利妥霉素类似物及其用途

    公开(公告)号：US07342011B2

    公开(公告)日：2008-03-11

    申请号：US10915919

    申请日：2004-08-11

    申请人： John H. van Duzer ,  Arthur F. Michaelis ,  William B. Geiss ,  Douglas G. Stafford ,  Joseph Raker

    发明人： John H. van Duzer ,  Arthur F. Michaelis ,  William B. Geiss ,  Douglas G. Stafford ,  Joseph Raker

    IPC分类号： C07D498/18 ,  A61K31/535 ,  A61P31/54

    CPC分类号： C07D498/18 ,  C07D491/18 ,  C07D513/18 ,  C07D519/00

    摘要： The present invention features rifamycin analogs that can be used as therapeutics for treating or preventing a variety of microbial infections. In one form, the analogs are acetylated at the 25-position, as is rifamycin. In another form, the analogs are deacetylated at the 25-position. In yet other forms, benzoxazinorifamycin, benzthiazinorifamycin, and benzdiazinorifamycin analogs are derivatized at various positions of the benzene ring, including 3′-hydroxy analogs, 4′- and/or 6′ halo and/or alkoxy analogs, and various 5′ substituents that incorporate a cyclic amine moiety.

    摘要翻译： 本发明的特征是利福霉素类似物可用作治疗或预防各种微生物感染的治疗剂。 在一种形式中，类似物在25位被乙酰化，就像利福霉素一样。 在另一种形式中，类似物在25位脱乙酰化。 在其他形式中，苯并恶嗪利霉素，苯并噻嗪可的霉素和苯并二氮霉素霉素类似物在苯环的各个位置衍生化，包括3'-羟基类似物，4'-和/或6'卤素和/或烷氧基类似物，以及各种5'取代基 加入环胺部分。