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1. 发明申请

WO2011123751A2 HETEROCYCLIC COMPOUNDS AND THEIR USES 审中-公开
公开(公告)号：WO2011123751A2
公开(公告)日：2011-10-06
申请号：PCT/US2011/030888
申请日：2011-04-01
申请人： AMGEN INC. , CUSHING, Timothy, D. , DUQUETTE, Jason, A. , HE, Xiao , LOHMAN, Julia, Winslow , SHIN, Youngsook
发明人： CUSHING, Timothy, D. , DUQUETTE, Jason, A. , HE, Xiao , LOHMAN, Julia, Winslow , SHIN, Youngsook
IPC分类号： C07D401/14 , C07D403/12 , C07D471/04 , C07D409/12 , C07D473/34 , C07D487/04 , A61K31/506 , A61P29/00
CPC分类号： C07D403/12 , C07D401/14 , C07D409/12 , C07D471/04 , C07D473/34 , C07D487/04
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 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 (B-ALL) Non Hodgkins Lymphoma (NHL) B-cell lymphoma and solid tumors, such as breast cancer.

2. 发明申请

WO2010151735A3 4H - PYRIDO [ 1, 2 - A] PYRIMIDIN - 4 - ONE DERIVATIVES AS PI3 K INHIBITORS 审中-公开
公开(公告)号：WO2010151735A3
公开(公告)日：2010-12-29
申请号：PCT/US2010/039931
申请日：2010-06-25
申请人： AMGEN INC. , CUSHING, Timothy D. , HAO, Xiaolin , LOHMAN, Julia Winslow , SHIN, Youngsook
发明人： CUSHING, Timothy D. , HAO, Xiaolin , LOHMAN, Julia Winslow , SHIN, Youngsook
IPC分类号： C07D401/12 , C07D471/04 , C07D473/34 , C07D473/38 , C07D487/04 , A61K31/52 , A61K31/517 , A61K31/506 , A61P29/00
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 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 (B-ALL) Non Hodgkins Lymphoma (NHL) B-cell lymphoma and solid tumors, such as breast cancer.

3. 发明申请

WO2011123751A3 HETEROCYCLIC COMPOUNDS AND THEIR USE AS PI3K INHIBITORS 审中-公开
标题翻译：杂环化合物及其作为PI3K抑制剂使用
公开(公告)号：WO2011123751A3
公开(公告)日：2014-08-07
申请号：PCT/US2011030888
申请日：2011-04-01
申请人： AMGEN INC , CUSHING TIMOTHY D , DUQUETTE JASON A , HE XIAO , LOHMAN JULIA WINSLOW , SHIN YOUNGSOOK
发明人： CUSHING TIMOTHY D , DUQUETTE JASON A , HE XIAO , LOHMAN JULIA WINSLOW , SHIN YOUNGSOOK
IPC分类号： C07D401/14 , A61K31/506 , A61P29/00 , C07D403/12 , C07D409/12 , C07D471/04 , C07D473/34 , C07D487/04
CPC分类号： C07D403/12 , C07D401/14 , C07D409/12 , C07D471/04 , C07D473/34 , C07D487/04
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 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 (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，如急性骨髓性白血病（AML）骨髓增生异常综合征（MDS）骨髓增殖性疾病（MPD）慢性骨髓性白血病（MPD），慢性骨髓性白血病 C ML）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。

4. 发明申请

WO2006044133A1 ACTIVE KETONE INHIBITORS OF TRYPTASE 审中-公开
标题翻译：活性酮酮抑制剂
公开(公告)号：WO2006044133A1
公开(公告)日：2006-04-27
申请号：PCT/US2005/034811
申请日：2005-09-26
申请人： AXYS PHARMACEUTICALS, INC. , CHEHADE, Kareem, A.H. , HIRSCHBEIN, Bernard, L. , LEE, Chang-sun , LIU, Weili , LOHMAN, Julia, Winslow , MENDONCA, Rohan, V. , PALMER, James, P. , SPENCER, Jeffrey, R. , SPERANDIO, David , SPRENGLER, Paul, A. , TAI, Vincent, w.-F.
发明人： CHEHADE, Kareem, A.H. , HIRSCHBEIN, Bernard, L. , LEE, Chang-sun , LIU, Weili , LOHMAN, Julia, Winslow , MENDONCA, Rohan, V. , PALMER, James, P. , SPENCER, Jeffrey, R. , SPERANDIO, David , SPRENGLER, Paul, A. , TAI, Vincent, w.-F.
IPC分类号： C07D271/06 , C07D413/12 , C07D471/04 , A61K31/4245 , A61P11/06
CPC分类号： C07D471/04 , C07D271/06 , C07D409/12 , C07D413/06 , C07D413/12
摘要： The present invention related to certain active tetracyclic ketone inhibitors of tryptase, pharmaceutical composition comprising these compounds and methods of treating asthma, allergic rhinitis, and/or Chronic Obstructive Pulmonary Disease utilizing these compounds.
摘要翻译：本发明涉及一些类胰蛋白酶的活性四环酮抑制剂，包含这些化合物的药物组合物以及利用这些化合物治疗哮喘，过敏性鼻炎和/或慢性阻塞性肺疾病的方法。

5. 发明申请

WO2010151737A3 HETEROCYCLIC COMPOUNDS AND THEIR USES AS INHIBITORS OF PI3 K ACTIVITY 审中-公开
标题翻译：杂环化合物及其作为PI3K活性抑制剂的用途
公开(公告)号：WO2010151737A3
公开(公告)日：2011-05-05
申请号：PCT/US2010039937
申请日：2010-06-25
申请人： AMGEN INC , BROWN MATTHEW , CHEN YI , CUSHING TIMOTHY D , GONZALEZ LOPEZ DE TURISO FELIX , HE XIAO , KOHN TODD J , LOHMAN JULIA WINSLOW , PATTAROPONG VATEE , SEGANISH JENNIFER , SHIN YOUNGSOOK , SIMARD JILLIAN L
发明人： BROWN MATTHEW , CHEN YI , CUSHING TIMOTHY D , GONZALEZ LOPEZ DE TURISO FELIX , HE XIAO , KOHN TODD J , LOHMAN JULIA WINSLOW , PATTAROPONG VATEE , SEGANISH JENNIFER , SHIN YOUNGSOOK , SIMARD JILLIAN L
IPC分类号： C07D401/14 , A61K31/4709 , A61K31/506 , A61K31/5377 , A61K31/538 , A61P29/00 , C07D413/14 , C07D417/14 , C07D471/04 , C07D473/00 , C07D491/107 , C07D491/113 , C07D491/20 , C07D495/10 , C07D513/04
CPC分类号： C07D401/14 , C07D413/14 , C07D417/14 , C07D471/04 , C07D473/00 , C07D491/107 , C07D491/113 , C07D491/20 , C07D495/10 , C07D513/04
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 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 (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，如急性骨髓性白血病（AML）骨髓增生异常综合征（MDS）骨髓增殖性疾病（MPD）慢性骨髓性白血病（MPD），慢性骨髓性白血病 C ML）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。

6. 发明申请

WO2010151735A2 HETEROCYCLIC COMPOUNDS AND THEIR USES 审中-公开
标题翻译：杂环化合物及其用途
公开(公告)号：WO2010151735A2
公开(公告)日：2010-12-29
申请号：PCT/US2010039931
申请日：2010-06-25
申请人： AMGEN INC , CUSHING TIMOTHY D , HAO XIAOLIN , LOHMAN JULIA WINSLOW , SHIN YOUNGSOOK
发明人： CUSHING TIMOTHY D , HAO XIAOLIN , LOHMAN JULIA WINSLOW , SHIN YOUNGSOOK
IPC分类号： C07D401/12 , A61K31/506 , A61K31/517 , A61K31/52 , A61P29/00 , C07D471/04 , C07D473/34 , C07D473/38 , C07D487/04
CPC分类号： C07D473/34 , C07D401/12 , C07D471/04 , C07D473/38 , C07D487/04
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 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 (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，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，如急性骨髓性白血病（AML）骨髓增生异常综合征（MDS）骨髓增殖性疾病（MPD）慢性骨髓性白血病（MPD），慢性骨髓性白血病 C ML）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。

7. 发明申请

WO2012068343A1 QUINOLINE DERIVATIVES AS PIK3 INHIBITORS 审中-公开
标题翻译：喹啉衍生物作为PIK3抑制剂
公开(公告)号：WO2012068343A1
公开(公告)日：2012-05-24
申请号：PCT/US2011/061141
申请日：2011-11-17
申请人： AMGEN INC. , CUSHING, Timothy D. , LOHMAN, Julia Winslow , SHIN, Youngsook
发明人： CUSHING, Timothy D. , LOHMAN, Julia Winslow , SHIN, Youngsook
IPC分类号： C07D401/14 , C07D413/14 , A61K31/506 , A61P35/00 , A61P29/00 , A61P37/00
CPC分类号： A61K31/506 , C07D239/42 , C07D401/14 , C07D413/14
摘要： Substituted bicyclic heteroaryls having the general formula (I) 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 p1 108 activity, including but not restricted to leukemias, such as Acute Myeloid leukaemia (AML), Myelodysplastic syndrome (MDS), myeio-proiiferative 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：具有通式（I）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，皮肤炎症组分慢性炎性病症，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，包括所有形式的过敏症状本发明还使得能够治疗依赖于p1108活性或与p1108活性相关的癌症的方法，所述癌症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），骨髓增生症疾病（MPD），慢性骨髓性白血病（CML），T细胞急性淋巴细胞白血病（T-ALL），B细胞急性淋巴细胞性白血病（B-ALL），非霍奇金淋巴瘤（NHL），B细胞淋巴瘤和实体瘤，如乳腺癌。

8. 发明申请

WO2010151737A2 HETEROCYCLIC COMPOUNDS AND THEIR USES 审中-公开
公开(公告)号：WO2010151737A2
公开(公告)日：2010-12-29
申请号：PCT/US2010/039937
申请日：2010-06-25
申请人： AMGEN INC. , BROWN, Matthew , CHEN, Yi , CUSHING, Timothy D. , GONZALEZ LOPEZ DE TURISO, Felix , HE, Xiao , KOHN, Todd J. , LOHMAN, Julia Winslow , PATTAROPONG, Vatee , SEGANISH, Jennifer , SHIN, Youngsook , SIMARD, Jillian L.
发明人： BROWN, Matthew , CHEN, Yi , CUSHING, Timothy D. , GONZALEZ LOPEZ DE TURISO, Felix , HE, Xiao , KOHN, Todd J. , LOHMAN, Julia Winslow , PATTAROPONG, Vatee , SEGANISH, Jennifer , SHIN, Youngsook , SIMARD, Jillian L.
IPC分类号： C07D401/14
CPC分类号： C07D401/14 , C07D413/14 , C07D417/14 , C07D471/04 , C07D473/00 , C07D491/107 , C07D491/113 , C07D491/20 , C07D495/10 , C07D513/04
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 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 (B-ALL) Non Hodgkins Lymphoma (NHL) B-cell lymphoma and solid tumors, such as breast cancer.

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