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1. 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.

2. 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。

3. 发明申请

WO2010077992A1 AMINOPYRIDINE AND CARBOXYPYRIDINE COMPOUNDS AS PHOSPHODIESTERASE 10 INHIBITORS 审中-公开
标题翻译：氨基吡啶和羧基吡啶化合物作为磷酸二酯酶10抑制剂
公开(公告)号：WO2010077992A1
公开(公告)日：2010-07-08
申请号：PCT/US2009/068330
申请日：2009-12-16
申请人： AMGEN INC. , ALLEN, Jennifer R. , CHEN, Ning , FALSEY, James R. , FROHN, Michael , HARRINGTON, Paul , HU, Essa , KALLER, Matthew R. , KUNZ, Roxanne , MERCEDE, Stephanie J. , NGUYEN, Thomas T. , PICKRELL, Alexander J. , REICHELT, Andreas , RUMFELT, Shannon , RZASA, Robert M. , SHAM, Kelvin , SIEGMUND, Aaron C. , TEGLEY, Christopher M. , YAO, Guomin
发明人： ALLEN, Jennifer R. , CHEN, Ning , FALSEY, James R. , FROHN, Michael , HARRINGTON, Paul , HU, Essa , KALLER, Matthew R. , KUNZ, Roxanne , MERCEDE, Stephanie J. , NGUYEN, Thomas T. , PICKRELL, Alexander J. , REICHELT, Andreas , RUMFELT, Shannon , RZASA, Robert M. , SHAM, Kelvin , SIEGMUND, Aaron C. , TEGLEY, Christopher M. , YAO, Guomin
IPC分类号： C07D213/74 , C07D213/84 , C07D401/12 , C07D401/14 , C07D407/14 , C07D409/14 , C07D413/14 , A61K31/444 , A61P25/18
CPC分类号： C07D401/04 , C07D213/74 , C07D213/84 , C07D401/12 , C07D401/14 , C07D407/14 , C07D409/14 , C07D413/14
摘要： Pyridine and pyrimidine compounds: (I); or a pharmaceutically acceptable salt thereof, wherein m, n, R 1 , R 2 , R 3 , R 4 , R 5 , R 6 , R 7 , X 1 , X 2 , X 3 , X 4 , X 5 , X 6 , X 7 , X 8 , and Y are as defined in the specification; (II); or a pharmaceutically acceptable salt thereof, wherein ring A, m, n, y, R 2 , R 3 , R 4 , R 5 , R 6 , R 7 , R 8 , R 9 , X 1 , X 2 , and ring A are as defined in the specification; and (III); or a pharmaceutically acceptable salt thereof, wherein m, n, y, R 2 , R 3 , R 4 , R 5 , R 6 , R 7 , R 9 , X 1 , X 2 , and ring A are as defined in the specification; 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：（I）; 或其药学上可接受的盐，其中m，n，R1，R2，R3，R4，R5，R6，R7，X1，X2，X3，X4，X5，X6，X7，X8和Y如本说明书 ; （II）; 或其药学上可接受的盐，其中环A，m，n，y，R 2，R 3，R 4，R 5，R 6，R 7，R 8，R 9，X 1，X 2和环A如说明书中所定义; 和（III）; 或其药学上可接受的盐，其中m，n，y，R2，R3，R4，R5，R6，R7，R9，X1，X2和环A如说明书中所定义; 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，双相性精神障碍，强迫症等。

4. 发明申请

WO2007124181A3 THIENO-[2,3-D]PYRIMIDINE AND THIENO-PYRIDAZINE COMPOUNDS AND METHODS OF USE 审中-公开
公开(公告)号：WO2007124181A3
公开(公告)日：2007-11-01
申请号：PCT/US2007/010093
申请日：2007-04-23
申请人： AMGEN INC. , HONG, Fang-Tsao , FALSEY, James R. , RZASA, Robert M. , TADESSE, Seifu , TASKER, Andrew
发明人： HONG, Fang-Tsao , FALSEY, James R. , RZASA, Robert M. , TADESSE, Seifu , TASKER, Andrew
IPC分类号： C07D495/04 , A61K31/519 , A61P29/00
摘要： The present invention comprises a new class of compounds useful for the prophylaxis and treatment of protein kinase mediated diseases, including inflammation and related conditions. The compounds have a general Formula (I), wherein A 1 , A 2 , B, R 2 and R 3 are defined herein. The invention also comprises pharmaceutical compositions including one or more compounds of Formula (I), uses of such compounds and compositions for treatment of kinase mediated diseases including rheumatoid arthritis, psoriasis and other inflammation disorders, as well as intermediates and processes useful for the preparation of compounds of Formula (I).

5. 发明申请

WO2005077944A1 PYRIMIDINE DERIVATIVES FOR USE AS VANILLOID RECEPTOR LIGANDS AND THEIR USE IN THE TREATMENT OF PAIN 审中-公开
标题翻译：用作VANILLOID受体配体的吡嗪衍生物及其在治疗疼痛中的应用
公开(公告)号：WO2005077944A1
公开(公告)日：2005-08-25
申请号：PCT/US2005/004378
申请日：2005-02-11
申请人： AMGEN INC.
发明人： WANG, Hui-Ling , BALAN, Chenera , DOHERTY, Elizabeth M. , FALSEY, James R. , GORE, Vijay Keshav , KATON, Jodie , NORMAN, Mark H.
IPC分类号： C07D417/12
CPC分类号： C07D401/12 , C07D403/12 , C07D405/12 , C07D413/12 , C07D417/12 , C07D417/14 , C07D471/04
摘要： Pyrimidine ethers and compositions containing them, fo use as vanilloid receptor ligands for the treatment of acute, inflammatory and neuropathic pain, dental pain, general headache, migraine, cluster headache, mixed-vascular and non-vascular syndromes, tension headache, 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, inflammatory pain and associated hyperalgesia and allodynia, neuropathic pain and associated hyperalgesia and allodynia, diabetic neuropathy pain, causalgia, sympathetically maintained pain, deafferentation syndromes, asthma, epithelial tissue damage or dysfunction, herpes simplex, disturbances of visceral motility at respiratory, genitourinary, gastrointestinal or vascular regions, wounds, burns, allergic skin reactions, pruritus, vitiligo, general gastrointestinal disorders, gastric ulceration, duodenal ulcers, diarrhea, gastric lesions induced by necrotising agents, hair growth, vasomotor or allergic rhinitis, bronchial disorders or bladder disorders. Wherein R 1 - R 4 and X are as defined in the claims.
摘要翻译：嘧啶醚和含有它们的组合物，用作治疗急性，炎性和神经性疼痛，牙痛，一般头痛，偏头痛，丛集性头痛，混合血管和非血管性综合征，紧张性头痛，一般炎症，关节炎，风湿性疾病，骨关节炎，炎症性肠病，炎症性眼病，炎性或不稳定性膀胱病，银屑病，皮肤炎症成分炎症，慢性炎性病症，炎性疼痛及相关的痛觉过敏和异常性疼痛，神经性疼痛及相关的痛觉过敏和异常性疼痛，糖尿病神经病痛，咳嗽痛，交感神经保持疼痛，交感综合征，哮喘，上皮组织损伤或功能障碍，单纯疱疹，呼吸道内脏运动性紊乱，泌尿生殖道，胃肠道或血管区，伤口，烧伤，过敏性皮肤反应，瘙痒，白癜风，一般 gastrointesti 鼻坏死症，胃溃疡，十二指肠溃疡，腹泻，坏死因子诱导的胃损伤，毛发生长，血管舒缩或过敏性鼻炎，支气管疾病或膀胱疾病。其中R 1至R 4和X如权利要求中所定义。

6. 发明申请

WO2014165277A2 POTENT AND SELECTIVE INHIBITORS OF Nav1.7 审中-公开
标题翻译： Nav1.7的POTENT和选择性抑制剂
公开(公告)号：WO2014165277A2
公开(公告)日：2014-10-09
申请号：PCT/US2014/025062
申请日：2014-03-12
申请人： AMGEN INC.
发明人： MURRAY, Justin K. , HOLDER, Jerry Ryan , WANSKA, Malgorzata , TEGLEY, Christopher M. , FALSEY, James R. , DOHERTY, Elizabeth M. , MIRANDA, Leslie P. , BISWAS, Kaustav , WU, Bin , SHAM, Kelvin , LONG, Jason C.
IPC分类号： C07K14/435
CPC分类号： C07K14/43518 , A61K38/00 , A61K38/1767 , A61K47/48284 , A61K47/48438 , A61K47/643 , A61K47/6817
摘要： Disclosed is a composition of matter comprising an isolated polypeptide, which is a peripherally-restricted Nav1.7 inhibitor. In some disclosed embodiments, the isolated polypeptide is an inhibitor of Nav1.7. Other embodiments are conjugated embodiments of the inventive composition of matter and pharmaceutical compositions containing the inventive composition of matter. Isolated nucleic acids encoding some embodiments of inventive polypeptides and expression vectors, and recombinant host cells containing them are disclosed. A method of treating or preventing pain is also disclosed.
摘要翻译：公开了包含分离的多肽的物质组合物，其是外周限制的Nav1.7抑制剂。在一些公开的实施方案中，分离的多肽是Nav1.7的抑制剂。其它实施方案是本发明组合物和包含本发明组合物的药物组合物的共轭实施方案。公开了编码本发明多肽和表达载体的一些实施方案的分离的核酸，以及含有它们的重组宿主细胞。还公开了治疗或预防疼痛的方法。

7. 发明申请

WO2019028382A1 METHOD OF CONJUGATION OF CYS-MABS 审中-公开
公开(公告)号：WO2019028382A1
公开(公告)日：2019-02-07
申请号：PCT/US2018/045212
申请日：2018-08-03
申请人： AMGEN INC.
发明人： ACHMATOWICZ, Michal , ROMANINI, Dante , FALSEY, James R. , HERBERICH, Bradley J. , THIEL, Oliver R.
IPC分类号： A61K47/68 , C07K16/00 , C07K14/605
摘要： The present disclosure relates to a method of capping, reducing, and oxidizing cys-mAbs in order to provide homogenous material for subsequent conjugation reactions. The present method demonstrates robust ways to manufacture conjugates of cysteine-engineered antibodies that offer high yield and consistent product quality.

8. 发明申请

WO2018136440A1 METHOD OF TREATING OR AMELIORATING METABOLIC DISORDERS USING GLP-1 RECEPTOR AGONISTS CONJUGATED TO ANTAGONISTS FOR GASTRIC INHIBITORY PEPTIDE RECEPTOR (GIPR) 审中-公开
公开(公告)号：WO2018136440A1
公开(公告)日：2018-07-26
申请号：PCT/US2018/013918
申请日：2018-01-16
申请人： AMGEN INC.
发明人： CHENG, Yuan , NETIROJJANAKUL, Chawita , HOLDER, Jerry Ryan , WU, Bin , FALSEY, James R. , HERBERICH, Bradley J. , SHAM, Kelvin , MIRANDA, Leslie P. , LU, Shu-Chen , VENIANT-ELLISON, Murielle M. , STANISLAUS, Shanaka , YIE, Junming , XU, Jing
IPC分类号： A61K39/395 , C07K16/28 , A61P3/10
摘要： Methods of treating metabolic diseases and disorders using a composition comprising an antigen binding protein specific for the GIPR polypeptide conjugated to a GLP-1 receptor agonist are provided. In various embodiments the metabolic disease or disorder is type 2 diabetes, obesity, dyslipidemia, elevated glucose levels, elevated insulin levels and diabetic nephropathy. In certain embodiments the composition comprises an antibody or functional fragment thereof comprising a cysteine at one or more conjugation site(s) wherein the GLP-1 receptor agonist is conjugated to the antibody or functional fragment thereof through the side-chain of the cysteine residue.

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