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1. 发明申请

WO2009011871A3 THIADIAZOLE MODULATORS OF PKB 审中-公开
公开(公告)号：WO2009011871A3
公开(公告)日：2009-01-22
申请号：PCT/US2008/008690
申请日：2008-07-15
申请人： AMGEN INC. , ALLEN, John, G. , BOURBEAU, Matthew, P. , DOMINGUEZ, Celia , FOTSCH, Christopher, H. , HAN, Nianhe , HONG, Fang-tsao , HUANG, Xin , LEE, Matthew, R. , LIU, Qingyian , REICHELT, Andreas , TADESSE, Seifu , WANG, Xianghong , YAO, Guomin , YUAN, Chester Chenguang , ZENG, Qingping
发明人： ALLEN, John, G. , BOURBEAU, Matthew, P. , DOMINGUEZ, Celia , FOTSCH, Christopher, H. , HAN, Nianhe , HONG, Fang-tsao , HUANG, Xin , LEE, Matthew, R. , LIU, Qingyian , REICHELT, Andreas , TADESSE, Seifu , WANG, Xianghong , YAO, Guomin , YUAN, Chester Chenguang , ZENG, Qingping
IPC分类号： C07D471/02 , C07D285/135 , C07D285/125 , A61K31/433 , A61P35/00 , A61P29/00
摘要： The invention relates to thiazole compounds of Formula I and Formula II and compositions thereof useful for treating diseases mediated by protein kinase B (PKB) where the variables have the definitions provided herein. The invention also relates to the therapeutic use of such thiazole compounds and compositions thereof in treating disease states associated with abnormal cell growth, cancer, inflammation, and metabolic disorders.

2. 发明申请

WO2008118468A1 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：WO2008118468A1
公开(公告)日：2008-10-02
申请号：PCT/US2008/003962
申请日：2008-03-24
申请人： AMGEN INC.
发明人： CHEN, Yi , CUSHING, Timothy D. , DUQUETTE, Jason A. , GONZALEZ LOPEZ DE TURISO, Felix , HAO, Xiaolin , HE, Xiao , LUCAS, Brian , MCGEE, Lawrence R. , REICHELT, Andreas , RZASA, Robert M. , SEGANISH, Jennifer , SHIN, Youngsook , ZHANG, Dawei
IPC分类号： C07D473/30 , C07D473/34 , C07D487/04 , A61K31/519 , A61K31/52 , A61P29/00 , A61P35/00
CPC分类号： C07D487/04 , C07D471/04 , C07D473/30 , C07D473/34
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性疾病如系统性红斑狼疮（SLE），重症肌无力，类风湿关节炎，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。本发明还能够治疗与p110活性介导，依赖或相关的癌症的方法，包括但不限于白血病，例如急性骨髓性白血病（AML），骨髓增生异常综合征（myelo-dysplastic syndrome，MDS），骨髓增殖性疾病（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。

3. 发明申请

WO2010057126A1 PYRIDINE AND PYRIMIDINE DERIVATIVES AS PHOSPHODIESTERASE 10 INHIBITORS 审中-公开
标题翻译：吡啶和吡嗪衍生物作为磷酸二酯酶10抑制剂
公开(公告)号：WO2010057126A1
公开(公告)日：2010-05-20
申请号：PCT/US2009/064643
申请日：2009-11-16
申请人： AMGEN INC. , ALLEN, Jennifer R. , BISWAS, Kaustav , CHAVEZ, Frank, Jr. , CHEN, Ning , DEMORIN, Frenel Fils , FALSEY, James R. , FROHN, Mike , HARRINGTON, Paul , HORNE, Dan , HU, Essa , KALLER, Matthew R. , KUNZ, Roxanne , MONENSCHEIN, Holger , NGUYEN, Tom , PICKRELL, Alex , REICHELT, Andreas , RUMFELT, Shannon , RZASA, Rob , SHAM, Kelvin , YAO, Guomin
发明人： ALLEN, Jennifer R. , BISWAS, Kaustav , CHAVEZ, Frank, Jr. , CHEN, Ning , DEMORIN, Frenel Fils , FALSEY, James R. , FROHN, Mike , HARRINGTON, Paul , HORNE, Dan , HU, Essa , KALLER, Matthew R. , KUNZ, Roxanne , MONENSCHEIN, Holger , NGUYEN, Tom , PICKRELL, Alex , REICHELT, Andreas , RUMFELT, Shannon , RZASA, Rob , SHAM, Kelvin , YAO, Guomin
IPC分类号： C07D401/12 , C07D401/14 , C07D417/12 , C07D471/04 , C07D473/00 , A61K31/4184 , A61P25/18 , A61P3/00
CPC分类号： C07D413/14 , C07D401/12 , C07D401/14 , C07D417/12 , C07D471/04 , C07D473/00
摘要： Pyridine and pyrimidine compounds, and compositions containing them, and processes for preparing such compounds. Provided herein also are methods of treating disorders or diseases treatable by inhibition of PDE10, such as obesity, non-insulin dependent diabetes, schizophrenia, bipolar disorder, obsessive-compulsive disorder, and the like.
摘要翻译：吡啶和嘧啶化合物，以及含有它们的组合物，以及制备这些化合物的方法。本文还提供治疗通过抑制PDE10可治疗的疾病或疾病的方法，例如肥胖症，非胰岛素依赖型糖尿病，精神分裂症，双相情感障碍，强迫症等。

4. 发明申请

WO2009011880A3 HETEROCYCLIC MODULATORS OF PKB 审中-公开
公开(公告)号：WO2009011880A3
公开(公告)日：2009-01-22
申请号：PCT/US2008/008723
申请日：2008-07-16
申请人： AMGEN INC. , ZENG, Qingping , ZHANG, Dawei , YAO, Guomin , WOHLHIETER, George E. , WANG, Xianghong , RIDER, James , REICHELT, Andreas , MONENSCHEIN, Holger , HONG, Fang-tsao , FALSEY, James R. , DOMINGUEZ, Celia , BOURBEAU, Matthew P. , ALLEN, John G.
发明人： ZENG, Qingping , ZHANG, Dawei , YAO, Guomin , WOHLHIETER, George E. , WANG, Xianghong , RIDER, James , REICHELT, Andreas , MONENSCHEIN, Holger , HONG, Fang-tsao , FALSEY, James R. , DOMINGUEZ, Celia , BOURBEAU, Matthew P. , ALLEN, John G.
IPC分类号： C07D263/48 , C07D401/04 , C07D403/04 , C07D413/04 , C07D413/14 , C07D417/04 , A61P35/00 , A61K31/5377 , A61K31/41
摘要： The invention relates to heterocyclic compounds of Formula I and compositions thereof useful for treating diseases mediated by protein kinase B (PKB) where the variables have the definitions provided herein Formula (I). The invention also relates to the therapeutic use of such compounds and compositions thereof in treating disease states associated with abnormal cell growth, cancer, inflammation, and metabolic disorders.

5. 发明申请

WO2008118454A2 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：WO2008118454A2
公开(公告)日：2008-10-02
申请号：PCT/US2008/003935
申请日：2008-03-24
申请人： AMGEN INC.
发明人： CHEN, Yi , CUSHING, Timothy D. , HAO, Xiaolin , HE, Xiao , REICHELT, Andreas , RZASA, Robert M. , SEGANISH, Jennifer , SHIN, Youngsook , ZHANG, Dawei
IPC分类号： C07D471/04 , C07D487/04 , A61K31/4985 , A61P9/00 , A61P19/02 , A61P37/00 , A61P35/00
CPC分类号： C07D487/04 , C07D471/04 , C07D519/00
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.
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

WO2012138776A1 BENZODIOXEPINE AND BENZODIOXINE COMPOUNDS THAT INTERACT WITH GLUCOKINASE REGULATORY PROTEIN FOR THE TREATMENT OF DIABETES 审中-公开
标题翻译：与葡萄糖激素调节蛋白质相互作用以治疗糖尿病的苯二酚和苯并二氧化锌化合物
公开(公告)号：WO2012138776A1
公开(公告)日：2012-10-11
申请号：PCT/US2012/032192
申请日：2012-04-04
申请人： AMGEN INC. , BARTBERGER, Michael, D. , CROGHAN, Michael, D. , FOTSCH, Christopher, H. , NORMAN, Mark, H. , PENNINGTON, Lewis, D. , REICHELT, Andreas , ST. JEAN, David, J., Jr. , TEGLEY, Christopher, M.
发明人： BARTBERGER, Michael, D. , CROGHAN, Michael, D. , FOTSCH, Christopher, H. , NORMAN, Mark, H. , PENNINGTON, Lewis, D. , REICHELT, Andreas , ST. JEAN, David, J., Jr. , TEGLEY, Christopher, M.
IPC分类号： C07D321/10 , C07D333/58 , C07D407/12 , C07D407/14 , C07D409/04 , C07D409/12 , C07D409/14 , C07D413/12 , C07D417/12 , C07D417/14 , C07D495/04 , C07D513/04 , A61K31/357 , A61K31/381 , A61K31/422
CPC分类号： A61K31/506 , A61K31/155 , A61K31/357 , A61K31/381 , A61K31/422 , A61K31/427 , A61K31/429 , A61K31/4365 , A61K31/443 , A61K31/4436 , A61K31/4709 , A61K45/06 , C07D321/10 , C07D333/58 , C07D405/14 , C07D407/12 , C07D407/14 , C07D409/04 , C07D409/12 , C07D409/14 , C07D413/12 , C07D417/12 , C07D417/14 , C07D495/04 , C07D513/04 , A61K2300/00
摘要： The present invention relates to compounds of formula I or II, or pharmaceutically acceptable salts thereof, that interact with glucokinase regulatory protein. In addition, the present invention relates to methods of treating type 2 diabetes, and other diseases and/or conditions where glucokinase regulatory protein is involved using the compounds, or pharmaceutically acceptable salts thereof, and pharmaceutical compositions that contain the compounds, or pharmaceutically acceptable salts thereof.
摘要翻译：本发明涉及与葡萄糖激酶调节蛋白相互作用的式I或II化合物或其药学上可接受的盐。此外，本发明还涉及治疗2型糖尿病的方法，以及使用该化合物或其药学上可接受的盐涉及葡萄糖激酶调节蛋白的其它疾病和/或病症，以及含有该化合物或其药学上可接受的盐的药物组合物它们。

7. 发明申请

WO2010083246A1 FLUOROISOQUINOLINE SUBSTITUTED THIAZOLE COMPOUNDS AND METHODS OF USE 审中-公开
标题翻译：氟代喹啉取代噻唑化合物及其使用方法
公开(公告)号：WO2010083246A1
公开(公告)日：2010-07-22
申请号：PCT/US2010/020938
申请日：2010-01-13
申请人： AMGEN INC. , ZENG, Qingping , YUAN, Chester Chenguang , YAO, Guomin , WANG, Xianghong , TADESSE, Seifu , ST. JEAN, JR., David J. , REICHELT, Andreas , LIU, Qingyian , HONG, Fang-Tsao , HAN, Nianhe , FOTSCH, Christopher H. , DAVIS, Carl D. , BOURBEAU, Matthew P. , ASHTON, Kate S. , ALLEN, John G.
发明人： ZENG, Qingping , YUAN, Chester Chenguang , YAO, Guomin , WANG, Xianghong , TADESSE, Seifu , ST. JEAN, JR., David J. , REICHELT, Andreas , LIU, Qingyian , HONG, Fang-Tsao , HAN, Nianhe , FOTSCH, Christopher H. , DAVIS, Carl D. , BOURBEAU, Matthew P. , ASHTON, Kate S. , ALLEN, John G.
IPC分类号： C07D409/04 , A61K31/427 , A61K31/4709
CPC分类号： C07D417/14 , C07D417/04
摘要： The invention relates to thiazole compounds of Formula (I) and compositions thereof useful for treating diseases mediated by protein kinase B (PKB) where the variables have the definitions provided herein. The invention also relates to the therapeutic use of such thiazole compounds and compositions thereof in treating disease states associated with abnormal cell growth, cancer, inflammation, and metabolic disorders.
摘要翻译：本发明涉及用于治疗由蛋白激酶B（PKB）介导的疾病的式（I）的噻唑化合物及其组合物，其中变量具有本文提供的定义。本发明还涉及这种噻唑化合物及其组合物治疗与异常细胞生长，癌症，炎症和代谢紊乱相关的疾病的治疗用途。

8. 发明申请

WO2008118455A1 δ3- SUBSTITUTED QUINOLINE OR QUINOXALINE DERIVATIVES AND THEIR USE AS PHOSPHATIDYLINOSITOL 3-KINASE ( PI3K) INHIBITORS 审中-公开
标题翻译： d3-取代的喹啉或喹喔啉衍生物及其作为磷酸胆碱3-激酶（PI3K）抑制剂的用途
公开(公告)号：WO2008118455A1
公开(公告)日：2008-10-02
申请号：PCT/US2008/003936
申请日：2008-03-24
申请人： AMGEN INC.
发明人： CHEN, Yi , CUSHING, Timothy D. , HAO, Xiaolin , HE, Xiao , REICHELT, Andreas , RZASA, Robert M. , SEGANISH, Jennifer , SHIN, Youngsook , ZHANG, Dawei
IPC分类号： C07D401/12 , C07D401/14 , A61K31/4709 , A61K31/506
CPC分类号： C07D401/12 , C07D401/14
摘要： Substituted bicyclic heteroaryls having the structure: (I) or any pharmaceutically-acceptable salt thereof, wherein: X 1 is C(R 9 ) or N; X 2 is C(R 10 ) or N; Y is N(R 11 ), O or S; which are useful to inhibit the biological activity of human PI3Kδ 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) myeloproliferative 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：具有以下结构的取代的双环杂芳基：（I）或其任何药学上可接受的盐，其中：X 1是C（R 9）或N; X 2是C（R 10）或N; Y是N（R 11），O或S; 其用于抑制人PI3Kd和含有它们的组合物的生物活性，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，皮肤炎症反应包括但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，过敏性疾病包括全部本发明还使得能够治疗依赖于p110d活性或与p110d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）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（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。

9. 发明申请

WO2013173382A1 BENZOTHIOPHENE SULFONAMIDES AND OTHER COMPOUNDS THAT INTERACT WITH GLUCOKINASE REGULATORY PROTEIN 审中-公开
标题翻译：苯并噻吩磺酰胺和与葡萄糖激酶调节蛋白相互作用的其他化合物
公开(公告)号：WO2013173382A1
公开(公告)日：2013-11-21
申请号：PCT/US2013/041011
申请日：2013-05-14
申请人： AMGEN INC.
发明人： ASHTON, Kate , BARTBERGER, Michael D. , BOURBEAU, Matthew Paul , CROGHAN, Michael D. , FOTSCH, Christopher H. , HUNGATE, Randall W. , KONG, Ke , NISHIMURA, Nobuko , NORMAN, Mark H. , PENNINGTON, Lewis D. , REICHELT, Andreas , SIEGMUND, Aaron C. , TADESSE, Seifu , ST. JEAN, David Jr , YANG, Kevin C. , YAO, Guomin
IPC分类号： C07D413/14 , C07D401/04 , C07D409/04 , C07D409/14 , C07D417/14 , C07D495/04 , A61K31/4365 , A61P5/50
CPC分类号： C07D409/04 , C07D401/04 , C07D409/14 , C07D413/14 , C07D417/14 , C07D495/04
摘要： The present invention relates to benzothiophene sulfonamides and other compounds that interact with glucokinase regulatory protein. In addition, the present invention relates to methods of treating type 2 diabetes, and other diseases and/or conditions where glucokinase regulatory protein is involved using the compounds, or pharmaceutically acceptable salts thereof, and pharmaceutical compositions that contain the compounds, or pharmaceutically acceptable salts thereof.
摘要翻译：本发明涉及苯并噻吩磺酰胺和与葡糖激酶调节蛋白相互作用的其它化合物。此外，本发明涉及治疗2型糖尿病的方法，以及其中使用所述化合物或其药学上可接受的盐涉及葡萄糖激酶调节蛋白的其它疾病和/或病症，以及含有所述化合物或其药学上可接受的盐的药物组合物它们。

10. 发明申请

WO2011143495A1 HETEROARYLOXYHETEROCYCLYL COMPOUNDS AS PDE10 INHIBITORS 审中-公开
标题翻译：作为PDE10抑制剂的异氟醚化合物
公开(公告)号：WO2011143495A1
公开(公告)日：2011-11-17
申请号：PCT/US2011/036342
申请日：2011-05-12
申请人： AMGEN INC. , ALLEN, Jennifer , HORNE, Daniel B. , HU, Essa , KALLER, Matthew R. , MONENSCHEIN, Holger , NGUYEN, Thomas T. , REICHELT, Andreas , RZASA, Robert M.
发明人： ALLEN, Jennifer , HORNE, Daniel B. , HU, Essa , KALLER, Matthew R. , MONENSCHEIN, Holger , NGUYEN, Thomas T. , REICHELT, Andreas , RZASA, Robert M.
IPC分类号： C07D401/14 , C07D403/14 , C07D405/14 , C07D417/14 , C07D471/04 , C07D471/08 , C07D487/10 , A61K31/4709 , A61K31/454 , A61K31/4535 , A61P25/18
CPC分类号： C07D491/107 , C07D401/04 , C07D401/06 , C07D401/14 , C07D403/04 , C07D403/14 , C07D405/04 , C07D405/14 , C07D409/14 , C07D413/14 , C07D417/14 , C07D471/04 , C07D471/08 , C07D487/04 , C07D487/10
摘要： Heteroaryloxyheterocyclyl compounds, and compositions containing them, and processes for preparing such compounds. Provided herein also are methods of treating disorders or diseases treatable by inhibition of PDE10, such as obesity, non-insulin dependent diabetes, schizophrenia, Huntington's Disease, bipolar disorder, obsessive-compulsive disorder, and the like.
摘要翻译：杂环氧基杂环基化合物和含有它们的组合物，以及这些化合物的制备方法。本文还提供治疗通过抑制PDE10可治疗的疾病或疾病的方法，例如肥胖症，非胰岛素依赖性糖尿病，精神分裂症，亨廷顿舞蹈病，双相情感障碍，强迫症等。

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