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1. 发明申请

WO2022115377A1 TRICYCLIC CARBOXAMIDE DERIVATIVES AS PRMT5 INHIBITORS 审中-公开
公开(公告)号：WO2022115377A1
公开(公告)日：2022-06-02
申请号：PCT/US2021/060332
申请日：2021-11-22
申请人： AMGEN INC.
发明人： AMEGADZIE, Albert , BEYLKIN, Diane Jennifer , BOOKER, Shon , BOURBEAU, Matthew Paul , BUTLER, John R. , GLAD, Sanne Omholt Schroder , KOHN, Todd J. , LANMAN, Brian Alan , LI, Kexue , LIU, Qingyian , LOPEZ, Patricia , MANONI, Francesco , NAVARATNE, Primali Vasundera , PETTUS, Liping H. , RAHIMOFF, Rene , TAMAYO, Nuria A. , VESTERGAARD, Mikkel , WANG, Hui-Ling , WEIRES, Nicholas Anthony
IPC分类号： C07D471/04 , A61K31/4355 , A61K31/437 , A61K31/501 , A61P35/00 , C07D491/048 , C07D491/147 , C07D471/14 , C07D498/04 , C07D401/14 , C07D401/12 , C07D495/04
摘要： Described herein are compounds of Formula (I) and pharmaceutically acceptable salts thereof, as well as pharmaceutical compositions thereof. Compounds of the present invention are useful for inhibiting PRMT5 activity and may have use in treating proliferative, such as cancer, metabolic and blood disorders. Compounds of Formula (I) have the following structure of Formule (I).

2. 发明申请

WO2021108404A1 HETEROCYCLIC COMPOUNDS AS DELTA-5 DESATURASE INHIBITORS AND METHODS OF USE 审中-公开
公开(公告)号：WO2021108404A1
公开(公告)日：2021-06-03
申请号：PCT/US2020/062011
申请日：2020-11-24
申请人： AMGEN INC.
发明人： ALLEN, Jennifer R. , AMEGADZIE, Albert , BOURBEAU, Matthew P. , CHEN, Ning , GOODMAN, Clifford , LATTANZI, Giulia , LINGARD, Iain , LIU, Qingyian , LOW, Jonathan D. , MA, Vu Van , MINATTI, Ana E. , POZZAN, Alfonso , REEVES, Corey , SIEGMUND, Aaron C. , TASSINI, Sabrina , TONELLI, Federica , WALTON, Mary
IPC分类号： C07D471/04 , A61K31/517 , A61K31/519 , C07D487/04 , C07D498/04 , A61P3/00 , A61P9/00
摘要： The present disclosure provides compounds useful for the inhibition of Delta-5 Desaturase ("D5D"). The compounds have a general Formula (I): wherein the variables of Formula (I) are defined herein. This disclosure also provides pharmaceutical compositions comprising the compounds, uses of the compounds, and compositions for treatment of, for example, a metabolic or cardiovascular disorder. Further, the disclosure provides intermediates useful in the synthesis of compounds of Formula (I).

3. 发明申请

WO2020132648A1 KIF18A INHIBITORS 审中-公开
公开(公告)号：WO2020132648A1
公开(公告)日：2020-06-25
申请号：PCT/US2019/068169
申请日：2019-12-20
申请人： AMGEN INC.
发明人： TAMAYO, Nuria A. , BANERJEE, Abhisek , BROWN, James Alexander , FROHN, Michael J. , CHEN, Jian Jeffrey , LI, Kexue , LIU, Qingyian , LOW, Jonathan Dante , MA, Vu , PETTUS, Liping H. , WALTON, Mary Catherine , MINATTI, Ana Elena , BOURBEAU, Matthew Paul , JIA, Lei
IPC分类号： A61P35/00 , C07D401/12 , C07D401/14 , C07D405/14 , C07D413/14 , A61K31/506 , C07D419/14 , C07D491/044
摘要： Compounds of formula (I): (I), as defined herein, and synthetic intermediates thereof, which are capable of modulating KIF18A protein thereby influencing the process of cell cycle and cell proliferation to treat cancer and cancer-related diseases. The invention also includes pharmaceutical compositions, including the compounds, and methods of treating disease states related to the activity of KIF18A.

4. 发明申请

WO2006019975A1 1,2,3,4-TETRAHYDROPYRAZIN-2-YL ACETAMIDES AND THEIR USE AS BRADYKININ ANTAGONISTS FOR THE TREATMENT OF INFLAMMATION RELATED DISORDERS 审中-公开
标题翻译： 1,2,3,4-四氢吡嗪-2-基乙酸酯及其用作治疗相关疾病的BRADYKININ拮抗剂
公开(公告)号：WO2006019975A1
公开(公告)日：2006-02-23
申请号：PCT/US2005/025090
申请日：2005-07-15
申请人： AMGEN INC.
发明人： ASKEW, JR., Benny C. , AYA, Toshihiro , BISWAS, Kaustav , CAI, Guolin , CHEN, Jian Jeffrey , HAN, Nianhe , LIU, Qingyian , NGUYEN, Thomas , NISHIMURA, Nobuko , NOMAK, Rana , PETERKIN, Tanya , QIAN, Wenyuan , YANG, Kevin , YUAN, Chester Chenguang , ZHU, Jiawang , D'AMICO, Derin C. , HUMAN, Jason Brooks , HUANG, QI
IPC分类号： C07D241/08
CPC分类号： C07D221/10 , C07D221/08 , C07D239/74 , C07D241/08 , C07D243/08 , C07D249/08 , C07D295/135 , C07D311/96 , C07D335/06 , C07D401/12 , C07D401/14 , C07D403/12 , C07D405/12 , C07D405/14 , C07D417/12 , C07D491/04
摘要： Selected compounds are effective for treatment of pain and diseases, such as inflammation mediated diseases. The invention encompasses novel compounds of formula (I) and pharmaceutically acceptable derivatives thereof, pharmaceutical compositions and methods for prophylaxis and treatment of diseases and other maladies or conditions involving pain, inflammation, and the like. The subject invention also relates to processes for making such compounds as well as to intermediates useful in such processes.
摘要翻译：所选化合物对于治疗疼痛和疾病如炎症介导的疾病是有效的。本发明包括式（I）的新型化合物及其药学上可接受的衍生物，用于预防和治疗疾病和其它疾病或涉及疼痛，炎症等的疾病的药物组合物和方法。本发明还涉及制备这些化合物的方法以及在这些方法中有用的中间体。

5. 发明申请

WO2022169948A1 TRICYCLIC-AMIDO-BICYCLIC PRMT5 INHIBITORS 审中-公开
公开(公告)号：WO2022169948A1
公开(公告)日：2022-08-11
申请号：PCT/US2022/015076
申请日：2022-02-03
申请人： AMGEN INC.
发明人： AMEGADZIE, Albert , BEYLKIN, Diane Jennifer , BOOKER, Shon , BOURBEAU, Matthew Paul , BUTLER, John R. , GREENMAN, Kevin Lloyd , KOHN, Todd J. , LI, Kexue , LIU, Qingyian , MINATTI, Ana Elena , NAVARATNE, Primali Vasundera , PETTUS, Liping H. , RAHIMOFF, Rene , WANG, Hui-Ling , WEIRES, Nicholas Anthony
IPC分类号： C07D471/04 , C07D471/14 , C07D491/048 , C07D491/052 , C07D491/147 , C07D495/04 , C07D498/04 , C07D519/00 , C07B59/00 , A61K31/55 , A61K31/4375 , A61K31/519 , A61K31/4355 , A61K31/437 , A61K31/4365 , A61P35/00
摘要： Described herein are novel PRMT5 inhibitors of Formula I and pharmaceutically acceptable salts thereof, as well as the pharmaceutical compositions thereof. Compounds of the present invention are useful for inhibiting PRMT5 activity and may have use in treating proliferative, metabolic and blood disorders. Compounds of Formula I have the following structure:

6. 发明申请

WO2014078314A1 AMINO-OXAZINE AND AMINO-DIHYDROTHIAZINE COMPOUNDS AS BETA-SECRETASE MODULATORS AND METHODS OF USE 审中-公开
标题翻译：氨基氧化胺和氨基二氢化合物作为β-分泌酶调节剂和使用方法
公开(公告)号：WO2014078314A1
公开(公告)日：2014-05-22
申请号：PCT/US2013/069697
申请日：2013-11-12
申请人： AMGEN INC.
发明人： WHITE, Ryan , EPSTEIN, Oleg , HUMAN, Jason, Brooks , ZHENG, Xiao Mei , SHAM, Kelvin , LIU, Qingyian , CHEN, Ning , CHENG, Yuan
IPC分类号： C07D498/10 , C07D498/20 , A61K31/537 , A61P25/28
CPC分类号： C07D519/00 , C07D311/80 , C07D491/052 , C07D498/10 , C07D498/20 , C07D513/10 , C07D513/20
摘要： The present invention comprises a new class of compounds useful for the modulation of Beta-secretase enzyme activity and for the treatment of Beta-secretase mediated diseases, including Alzheimer's disease (AD) and related conditions. In one embodiment, the compounds have a general Formula I wherein A 1, A 2 , A 3 , A 4 , A 5 , A 6 , L, R 2 , R 7 , X, Y and Z of Formula I are defined herein. The invention also includes use of these compounds in pharmaceutical compositions for treatment, prophylactic or therapeutic, of disorders and conditions related to the activity of beta-secretase protein. Such disorders include, for example, Alzheimer's Disease, cognitive deficits, cognitive impairment, schizophrenia and other central nervous system conditions related to and/or caused by the formation and/or deposition of plaque on the brain. The invention also comprises further embodiments of Formula I, intermediates and processes useful for the preparation of compounds of Formula I.
摘要翻译：本发明包括可用于调节β-分泌酶酶活性和用于治疗β-分泌酶介导的疾病（包括阿尔茨海默病（AD））和相关病症的新一类化合物。在一个实施方案中，化合物具有通式I，其中式I中的A1，A2，A3，A4，A5，A6，L，R2，R7，X，Y和Z如本文所定义。本发明还包括在药物组合物中用于治疗，预防或治疗与β-分泌酶蛋白活性相关的疾病和病症的用途。这种病症包括例如阿尔茨海默氏病，认知缺陷，认知障碍，精神分裂症和与脑上形成和/或沉积斑块相关和/或引起的其他中枢神经系统病症。本发明还包括式I的其它实施方案，可用于制备式I化合物的中间体和方法。

7. 发明申请

WO2013188724A1 AZETIDINE AND PIPERIDINE COMPOUNDS USEFUL AS PDE10 INHIBITORS 审中-公开
标题翻译：阿司匹林和哌啶化合物作为PDE10抑制剂有用
公开(公告)号：WO2013188724A1
公开(公告)日：2013-12-19
申请号：PCT/US2013/045768
申请日：2013-06-14
申请人： AMGEN INC.
发明人： ALLEN, Jennifer R. , CHEN, Jian J. , FROHN, Michael J. , KALLER, Matthew Richard , LIU, Qingyian , NGUYEN, Thomas T. , PICKRELL, Alexander J. , QIAN, Wenyuan , RZASA, Robert M. , ZHONG, Wenge
IPC分类号： C07D401/14 , C07D403/14 , A61K31/497 , A61P25/00
CPC分类号： C07D471/04 , A61K31/497 , A61K31/517 , A61K45/06 , C07D401/04 , C07D401/14 , C07D403/04 , C07D403/14
摘要： Azetidine and piperidine compounds of formula (I) as defined in the specification, compositions containing them, and processes for preparing such compounds and intermediates thereof. Provided herein also are methods of treating cognitive disorders or diseases treatable by inhibition of PDE10, such as Huntington's Disease, schizophrenia, bipolar disorder, obsessive-compulsive disorder, and the like.
摘要翻译：说明书中定义的式（I）的氮杂环丁烷和哌啶化合物，含有它们的组合物，以及制备这些化合物的方法及其中间体。本文还提供治疗认知障碍或通过抑制PDE10可治疗的疾病的方法，例如亨廷顿病，精神分裂症，双相障碍，强迫症等。

8. 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.

9. 发明申请

WO2004072068A1 VANILLOID RECEPTOR LIGANDS AND THEIR USE IN TREATMENTS 审中-公开
标题翻译： VANILLOID受体配体及其在治疗中的应用
公开(公告)号：WO2004072068A1
公开(公告)日：2004-08-26
申请号：PCT/US2004/003908
申请日：2004-02-09
申请人： AMGEN INC.
发明人： DOHERTY, Elizabeth, M. , HAN, Nianhe , HUNGATE, Randall, W. , LIU, Qingyian , NORMAN, Mark, H. , XI, Ning , XU, Shimin , FOTSCH, Christopher, H.
IPC分类号： C07D417/04
CPC分类号： C07D233/90 , C07D263/34 , C07D277/56 , C07D403/04 , C07D413/04 , C07D417/04 , C07D417/12 , C07D417/14
摘要： Compounds having the general structure and compositions containing them, 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.
摘要翻译：具有一般结构和含有它们的组合物的化合物，用于治疗急性，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，炎症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，糖尿病性神经病疼痛，咳嗽痛，交感神经痛，交感综合症，哮喘，上皮组织损伤或功能障碍，单纯疱疹，呼吸系统内脏运动紊乱，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， G 腹部溃疡，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。

10. 发明申请

WO2003009850A1 SUBSTITUTED PIPERAZINES AS MODULATORS OF THE MELANOCORTIN RECEPTOR 审中-公开
标题翻译：作为MELANOCORTIN受体的调节剂的替代哌啶
公开(公告)号：WO2003009850A1
公开(公告)日：2003-02-06
申请号：PCT/US2002/023926
申请日：2002-07-25
申请人： AMGEN INC.
发明人： FOTSCH, Christopher, H. , ARASASINGHAM, Premilla , BO, Yunxin , CHEN, Ning , GOLDBERG, Martin, H. , HAN, Nianhe , HSIEH, Feng-Yin , KELLY, Michael, G. , LIU, Qingyian , NORMAN, Mark, H. , SMITH, Duncan, M. , STEC, Markian , TAMAYO, Nuria , XI, Ning , XU, Shimin
IPC分类号： A61K31/495
CPC分类号： C07D207/08 , A61K38/00 , C07D205/04 , C07D207/09 , C07D209/14 , C07D209/42 , C07D211/26 , C07D211/60 , C07D211/62 , C07D213/38 , C07D213/81 , C07D213/82 , C07D215/48 , C07D217/06 , C07D217/14 , C07D217/26 , C07D233/64 , C07D295/185 , C07D317/60 , C07D317/68 , C07D319/18 , C07D401/12 , C07D403/12 , C07D409/12 , C07D413/12 , C07D417/12 , C07D451/02 , C07K5/06026 , C07K5/06139 , C07K5/06147 , C07K5/06191
摘要： Selected substituted piperazine compounds are effective for prophylaxis and treatment of diseases, such as obesity and the like. The invention encompasses novel compounds, analogs, prodrugs and pharmaceutically acceptable salts thereof, pharmaceutical compositions and methods for prophylaxis and treatment of diseases and other maladies or conditions involving activation of the melanocortin receptor. The subject invention also relates to processes For making such compounds as well as to intermediates useful in such processes.
摘要翻译：所选的取代哌嗪化合物对于预防和治疗诸如肥胖症等疾病是有效的。本发明包括新颖的化合物，类似物，前药和药学上可接受的盐，用于预防和治疗涉及黑皮质素受体活化的疾病和其它疾病或病症的药物组合物和方法。本发明还涉及制备这种化合物以及可用于这些方法的中间体的方法。

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