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    HETEROCYCLIC COMPOUNDS AND THEIR USES
    1.
    发明申请
    HETEROCYCLIC COMPOUNDS AND THEIR USES 有权
    杂环化合物及其用途

    公开(公告)号：US20100331293A1

    公开(公告)日：2010-12-30

    申请号：US12823767

    申请日：2010-06-25

    申请人： Timothy D. Cushing ,  Paul John Dransfield ,  Felix Gonzalez Lopez De Turiso ,  Michael G. Johnson ,  Todd Kohn ,  Vatee Pattaropong ,  Jillian L. Simard

    发明人： Timothy D. Cushing ,  Paul John Dransfield ,  Felix Gonzalez Lopez De Turiso ,  Michael G. Johnson ,  Todd Kohn ,  Vatee Pattaropong ,  Jillian L. Simard

    IPC分类号： A61K31/5377 ,  A61K31/541 ,  A61K31/506 ,  A61K31/4709 ,  C07D417/14 ,  C07D413/14 ,  C07D401/14 ,  A61P35/00 ,  A61P19/02 ,  A61P29/00 ,  A61P37/00

    CPC分类号： C07D401/04 ,  C07D215/44 ,  C07D401/12 ,  C07D401/14 ,  C07D407/14 ,  C07D409/12 ,  C07D413/14 ,  C07D417/14 ,  C07D471/04

    摘要： Substituted bicyclic heteroaryls and compositions containing them, for the treatment of general inflammation, arthritis, rheumatic diseases, osteoarthritis, inflammatory bowel disorders, inflammatory eye disorders, inflammatory or unstable bladder disorders, psoriasis, skin complaints with inflammatory components, chronic inflammatory conditions, including but not restricted to autoimmune diseases such as systemic lupus erythematosis (SLE), myestenia gravis, rheumatoid arthritis, acute disseminated encephalomyelitis, idiopathic thrombocytopenic purpura, multiples sclerosis, Sjogren's syndrome and autoimmune hemolytic anemia, allergic conditions including all forms of hypersensitivity, The present invention also enables methods for treating cancers that are mediated, dependent on or associated with p110δ activity, including but not restricted to leukemias, such as Acute Myeloid leukaemia (AML) Myelo-dysplastic syndrome (MDS) myelo-proliferative diseases (MPD) Chronic Myeloid Leukemia (CML) T-cell Acute Lymphoblastic leukaemia (T-ALL) B-cell Acute Lymphoblastic leukaemia (B-ALL) Non Hodgkins Lymphoma (NHL) B-cell lymphoma and solid tumors, such as breast cancer.

    摘要翻译： 取代的双环杂芳基和含有它们的组合物，用于治疗一般炎症，关节炎，风湿性疾病，骨关节炎，炎性肠病，炎症性眼病，炎症性或不稳定性膀胱病，牛皮癣，皮肤炎症成分的投诉，慢性炎性病症 不限于自身免疫性疾病如系统性红斑狼疮（SLE），重症肌无力，类风湿性关节炎，急性播散性脑脊髓炎，特发性血小板减少性紫癜，多发性硬化症，干燥综合征和自身免疫性溶血性贫血，包括所有形式的超敏反应的过敏症状 包括但不限于白血病，例如急性骨髓性白血病（AML）骨髓增生异常综合征（MDS）骨髓增生性疾病（MPD）慢性骨髓性白血病（MPD）慢性骨髓性白血病（MPD）的介导，依赖或与p110δ活性相关的癌症的方法 CML）T细胞急性淋巴细胞白血病（T-ALL）B细胞急性淋巴细胞白血病（B-ALL）非霍奇金淋巴瘤（NHL）B细胞淋巴瘤和实体瘤如乳腺癌。

    HETEROCYCLIC COMPOUNDS AND THEIR USES
    2.
    发明申请
    HETEROCYCLIC COMPOUNDS AND THEIR USES 审中-公开
    杂环化合物及其用途

    公开(公告)号：US20130079342A1

    公开(公告)日：2013-03-28

    申请号：US13701912

    申请日：2011-06-30

    申请人： Paul John Dransfield ,  Felix Gonzalez Lopez De Turiso ,  Vatee Pattaropong ,  Jillian L. Simard

    发明人： Paul John Dransfield ,  Felix Gonzalez Lopez De Turiso ,  Vatee Pattaropong ,  Jillian L. Simard

    IPC分类号： C07D413/14

    CPC分类号： C07D413/14 ,  C07D401/14 ,  C07D473/16

    摘要： Substituted bicyclic heteroaryls of the following formulae and compositions containing them, for the treatment of general inflammation, arthritis, rheumatic diseases, osteoarthritis, inflammatory bowel disorders, inflammatory eye disorders, inflammatory or unstable bladder disorders, psoriasis, skin complaints with inflammatory components, chronic inflammatory conditions, including but not restricted to autoimmune diseases such as systemic lupus erythematosis (SLE), myestenia gravis, rheumatoid arthritis, acute disseminated encephalomyelitis, idiopathic thrombocytopenic purpura, multiples sclerosis, Sjoegren's syndrome and autoimmune hemolytic anemia, allergic conditions including all forms of hypersensitivity, The present invention also enables methods for treating cancers that are mediated, dependent on or associated with p110 activity, including but not restricted to leukemias, such as Acute Myeloid leukaemia (AML) Myelo-dysplastic syndrome (MDS) myelo-proliferative diseases (MPD) Chronic Myeloid Leukemia (CML) T-cell Acute Lymphoblastic leukaemia (T-ALL) B-cell Acute Lymphoblastic leukaemia ALL) Non Hodgkins Lymphoma (NHL) B-cell lymphoma and solid tumors, such as breast cancer.

    摘要翻译： 下列配方的取代的双环杂芳基和含有它们的组合物，用于治疗一般炎症，关节炎，风湿性疾病，骨关节炎，炎性肠病，炎症性眼病，炎性或不稳定性膀胱病，牛皮癣，皮肤炎症成分的投诉，慢性炎症 包括但不限于自身免疫疾病如系统性红斑狼疮（SLE），重症肌无力，类风湿性关节炎，急性播散性脑脊髓炎，特发性血小板减少性紫癜，多发性硬化症，Sjoegren综合征和自身免疫性溶血性贫血，包括所有形式的超敏反应的过敏性疾病， 本发明还使得能够治疗依赖于p110活性或与p110活性相关的癌症的方法，包括但不限于白血病，例如急性骨髓性白血病（AML）Myelo-dysplastic综合征（MDS）骨髓增殖性疾病（MPD） C 慢性骨髓性白血病（CML）T细胞急性淋巴细胞白血病（T-ALL）B细胞急性淋巴细胞白血病ALL）非霍奇金淋巴瘤（NHL）B细胞淋巴瘤和实体瘤，如乳腺癌。

    Tricyclic inhibitors of hydroxysteroid dehydrogenases
    6.
    发明授权
    Tricyclic inhibitors of hydroxysteroid dehydrogenases 失效
    羟基类固醇脱氢酶的三环抑制剂

    公开(公告)号：US08765788B2

    公开(公告)日：2014-07-01

    申请号：US12664137

    申请日：2008-06-11

    申请人： Jay P. Powers ,  Daqing Sun ,  Xuelei Yan ,  Lisa Julian ,  Felix Gonzalez Lopez De Turiso

    发明人： Jay P. Powers ,  Daqing Sun ,  Xuelei Yan ,  Lisa Julian ,  Felix Gonzalez Lopez De Turiso

    IPC分类号： A61K31/445 ,  A61K31/425 ,  A61K31/42

    CPC分类号： C07D231/10 ,  C07D261/06 ,  C07D263/30 ,  C07D277/20

    摘要： The present invention provides tricyclic compounds according to formula (I): (I) where R1, R2, R3, W, X, Y, Z, m, n, and p are as defined in the description; as well as pharmaceutical compositions comprising the same, methods of use of the compounds and compositions of the invention for the treatment of conditions associated with hydroxysteroid dehydrogenases (e.g., 11-HSD1), and the use of the compounds of the invention in the preparation of medicaments for the treatment of hydroxysteroid dehydrogenase-associated conditions.

    摘要翻译： 本发明提供式（I）的三环化合物：（I）其中R 1，R 2，R 3，W，X，Y，Z，m，n和p如说明书中所定义; 以及包含其的药物组合物，使用本发明化合物和组合物的方法用于治疗与羟类固醇脱氢酶（例如，11-HSD1）相关的病症的用途，以及本发明化合物在制备 用于治疗羟基类固醇脱氢酶相关病症的药物。

    Heterocyclic compounds and their uses
    9.
    发明授权
    Heterocyclic compounds and their uses 失效
    杂环化合物及其用途

    公开(公告)号：US08633313B2

    公开(公告)日：2014-01-21

    申请号：US12971293

    申请日：2010-12-17

    申请人： Timothy David Cushing ,  Felix Gonzalez Lopez De Turiso ,  Xiaolin Hao ,  Youngsook Shin

    发明人： Timothy David Cushing ,  Felix Gonzalez Lopez De Turiso ,  Xiaolin Hao ,  Youngsook Shin

    IPC分类号： C07D403/12 ,  C07D403/14 ,  C07D487/04 ,  A61K31/506 ,  A61P19/02

    CPC分类号： C07D519/00 ,  C07D471/04

    摘要： Substituted bicyclic heteroaryls and compositions containing them, for the treatment of general inflammation, arthritis, rheumatic diseases, osteoarthritis, inflammatory bowel disorders, inflammatory eye disorders, inflammatory or unstable bladder disorders, psoriasis, skin complaints with inflammatory components, chronic inflammatory conditions, including but not restricted to autoimmune diseases such as systemic lupus erythematosis (SLE), myestenia gravis, rheumatoid arthritis, acute disseminated encephalomyelitis, idiopathic thrombocytopenic purpura, multiples sclerosis, Sjoegren's syndrome and autoimmune hemolytic anemia, allergic conditions including all forms of hypersensitivity, The present invention also enables methods for treating cancers that are mediated, dependent on or associated with p110δ activity, including but not restricted to leukemias, such as Acute Myeloid leukaemia (AML) Myelo-dysplastic syndrome (MDS) myelo-proliferative diseases (MPD) Chronic Myeloid Leukemia (CML) T-cell Acute Lymphoblastic leukaemia (T-ALL) B-cell Acute Lymphoblastic leukaemia (B-ALL) Non Hodgkins Lymphoma (NHL) B-cell lymphoma and solid tumors, such as breast cancer.

    摘要翻译： 取代的双环杂芳基和含有它们的组合物，用于治疗一般炎症，关节炎，风湿性疾病，骨关节炎，炎性肠病，炎症性眼病，炎症性或不稳定性膀胱病，牛皮癣，皮肤炎症成分的投诉，慢性炎性病症 不限于自身免疫疾病如系统性红斑狼疮（SLE），重症肌无力，类风湿性关节炎，急性播散性脑脊髓炎，特发性血小板减少性紫癜，多发性硬化症，Sjoegren综合征和自身免疫性溶血性贫血，包括所有形式的超敏反应的过敏症状 包括但不限于白血病，例如急性骨髓性白血病（AML）骨髓增生异常综合征（MDS）骨髓增生性疾病（MPD）慢性骨髓性白血病（Myeloid Leukem）的介导，依赖于或与p110delta活性相关的癌症的方法 ia（CML）T细胞急性淋巴细胞白血病（T-ALL）B细胞急性淋巴细胞白血病（B-ALL）非霍奇金淋巴瘤（NHL）B细胞淋巴瘤和实体瘤如乳腺癌。