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1. 发明申请

WO2010030954A1 SPIRO-TETRACYCLIC RING COMPOUNDS AS BETASECRETASE MODULATORS AND METHODS OF USE 审中-公开
标题翻译： SPIRO-TETRACYCLING环化合物作为BETASECRETASE调节剂和使用方法
公开(公告)号：WO2010030954A1
公开(公告)日：2010-03-18
申请号：PCT/US2009/056748
申请日：2009-09-11
申请人： AMGEN INC. , WHITE, Ryan , AMEGADZIE, Albert , BRYAN, Marian C. , CHEN, Jian J. , CHENG, Alan C. , DINEEN, Thomas , EPSTEIN, Oleg , GORE, Vijay Keshav , HUA, Zihao , HUMAN, Jason B. , HUANG, Hongbing , KREIMAN, Charles , LA, Daniel , LIU, Qingyian , MA, Vu Van , MARX, Isaac , PATEL, Vinod F. , QIAN, Wenyuan , WEISS, Matthew , YUAN, Chester C.
发明人： WHITE, Ryan , AMEGADZIE, Albert , BRYAN, Marian C. , CHEN, Jian J. , CHENG, Alan C. , DINEEN, Thomas , EPSTEIN, Oleg , GORE, Vijay Keshav , HUA, Zihao , HUMAN, Jason B. , HUANG, Hongbing , KREIMAN, Charles , LA, Daniel , LIU, Qingyian , MA, Vu Van , MARX, Isaac , PATEL, Vinod F. , QIAN, Wenyuan , WEISS, Matthew , YUAN, Chester C.
IPC分类号： C07D498/10 , C07D513/10 , A61K31/424 , A61K31/429 , A61P25/28
CPC分类号： C07D498/10 , C07D513/10
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 , T 1 , T 2 , W, 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）; 其中本文定义式（I）的A1，A2，A3，A4，A5，A6，T1，T2，W，X，Y和Z。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。

2. 发明申请

WO2009073203A1 TRP-M8 RECEPTOR LIGANDS AND THEIR USE IN TREATMENTS 审中-公开
标题翻译： TRP-M8受体配体及其在治疗中的应用
公开(公告)号：WO2009073203A1
公开(公告)日：2009-06-11
申请号：PCT/US2008/013375
申请日：2008-12-04
申请人： AMGEN INC. , NORMAN, Mark H. , BO, Yunxin Y. , GORE, Vijay Keshav , HORNE, Daniel , KALLER, Matthew , MA, Vu Van , MONENSCHEIN, Holger , NGUYEN, Thomas , NISHIMURA, Nobuko , TAMAYO, Nuria
发明人： NORMAN, Mark H. , BO, Yunxin Y. , GORE, Vijay Keshav , HORNE, Daniel , KALLER, Matthew , MA, Vu Van , MONENSCHEIN, Holger , NGUYEN, Thomas , NISHIMURA, Nobuko , TAMAYO, Nuria
IPC分类号： C07D217/04 , C07D217/06 , C07D217/22 , C07D401/04 , C07D401/06 , C07D401/10 , C07D401/12 , C07D405/06 , C07D405/12 , C07D413/06 , C07D417/06 , A61K31/472 , A61P29/00
CPC分类号： C07D217/04 , C07D217/06 , C07D217/22 , C07D401/04 , C07D401/06 , C07D401/10 , C07D401/12 , C07D405/06 , C07D405/12 , C07D413/06 , C07D417/06
摘要： Tetrahydroisoquinoline compounds of formula (I), and compositions containing them, for the treatment of acute, inflammatory and neurophatic 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, neurophatic pain and associated hyperalgesia and allodynia, diabetic neuropathy pain, causalgia, sympathetically maintened 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：式（I）的四氢异喹啉化合物和含有它们的组合物，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，炎性或不稳定性膀胱病，牛皮癣，皮肤炎症成分投诉，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，胃肠道消化胃溃疡，十二指肠溃疡，腹泻，坏死因子诱发的胃损伤，毛发生长，血管舒缩或过敏性鼻炎，支气管疾病或膀胱疾病。

3. 发明申请

WO2004035549A1 BENZIMIDAZOLE DERIVATIVES AND THEIR USE AS VANILLOID RECEPTOR LIGANDS 审中-公开
标题翻译：苯并咪唑衍生物及其作为VANILLOID受体配体使用
公开(公告)号：WO2004035549A1
公开(公告)日：2004-04-29
申请号：PCT/US2003/032823
申请日：2003-10-16
申请人： AMGEN INC. , BALAN, Chenera , BO, Yunxin , DOMINGUEZ, Celia , FOTSCH, Christopher, H. , GORE, Vijay, K. , MA, Vu Van , NORMAN, Mark, H. , OGNYANOV, Vassil, I. , QIAN, Yi-xin , WANG, Xianghong , XI, Ning , XU, Shimin
发明人： BALAN, Chenera , BO, Yunxin , DOMINGUEZ, Celia , FOTSCH, Christopher, H. , GORE, Vijay, K. , MA, Vu Van , NORMAN, Mark, H. , OGNYANOV, Vassil, I. , QIAN, Yi-xin , WANG, Xianghong , XI, Ning , XU, Shimin
IPC分类号： C07D235/30
CPC分类号： C07D401/04 , C07D235/30 , C07D401/12 , C07D401/14 , C07D403/12 , C07D403/14 , C07D405/14 , C07D409/14 , C07D417/12 , C07D417/14 , C07D471/04
摘要： Compounds of formula (I) are useful in the treatment of vanilloid-receptor-meditated diseases, such as inflammatory or neuropathic pain and diseases involving sensory nerve function such as asthma, rheumatoid arthritis, osteoarthritis, inflammatory bowel disorders, urinary incontinence, migraine and psoriasis.
摘要翻译：式（I）化合物可用于治疗香草素受体冥想疾病，例如炎性或神经性疼痛以及涉及感觉神经功能的疾病如哮喘，类风湿性关节炎，骨关节炎，炎性肠病，尿失禁，偏头痛和牛皮癣。

4. 发明申请

WO2006044527A1 IMIDAZOLE DERIVATIVES AS VANILLOID RECEPTOR LIGANDS 审中-公开
标题翻译：咪唑衍生物作为VANILLOID受体配体
公开(公告)号：WO2006044527A1
公开(公告)日：2006-04-27
申请号：PCT/US2005/036800
申请日：2005-10-14
申请人： AMGEN INC.
发明人： GORE, Vijay Keshav , MA, Vu Van , NORMAN, Mark H. , OGNYANOV, Vassil I. , XI, Ning
IPC分类号： C07D401/12 , C07D233/88 , A61K31/4168 , A61P29/00
CPC分类号： C07D233/64 , C07D401/12
摘要： Therapeutic benzimidazoles 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：治疗性苯并咪唑和含有它们的组合物，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，灼痛，交感神经痛维持疼痛，输血综合征，哮喘，上皮组织损伤或功能障碍，单纯疱疹，呼吸道，泌尿生殖道，胃肠道或血管区内脏运动紊乱，伤口，烧伤，过敏性皮肤反应，瘙痒，白癜风，一般胃肠道疾病，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。

5. 发明申请

WO2021163344A1 NOVEL PRMT5 INHIBITORS 审中-公开
公开(公告)号：WO2021163344A1
公开(公告)日：2021-08-19
申请号：PCT/US2021/017682
申请日：2021-02-11
申请人： AMGEN INC.
发明人： ALLEN, Jennifer Rebecca , AMEGADZIE, Albert , BEYLKIN, Diane Jennifer , BOOKER, Shon , BOURBEAU, Matthew Paul , BUTLER, John R. , FROHN, Michael J. , GLAD, Sanne Ormholt Schroder , HUSEMOEN, Birgitte Weinreich , KALLER, Matthew R. , KOHN, Todd J. , LANMAN, Brian Alan , LI, Kexue , LIU, Qingyian , LOPEZ, Patricia , MA, Vu Van , MANONI, Francesco , MEDINA, Jose , MINATTI, Ana Elena , PEIRO CADAHIA, Jorge , PETTUS, Liping , PICKRELL, Alexander J. , SARVARY, Ian , TAMAYO, Nuria A. , VESTERGAARD, Mikkel
IPC分类号： C07D401/12 , C07D401/14 , C07D403/12 , C07D405/14 , C07D413/14 , C07D417/14 , A61P35/00 , A61K31/435
摘要： Described herein are compounds of Formula I and pharmaceutically acceptable salt thereof, stereoisomers, tautomers as well as 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: (I)

6. 发明申请

WO2019213516A1 KRAS G12C INHIBITORS AND METHODS OF USING THE SAME 审中-公开
公开(公告)号：WO2019213516A1
公开(公告)日：2019-11-07
申请号：PCT/US2019/030593
申请日：2019-05-03
申请人： AMGEN INC.
发明人： ALLEN, John Gordon , ALLEN, Jennifer Rebecca , MINATTI, Ana Elena , XUE, Qiufen , WURZ, Ryan Paul , TEGLEY, Christopher M. , PICKRELL, Alexander J. , NGUYEN, Thomas T. , MA, Vu Van , LOPEZ, Patricia , LIU, Longbin , KOPECKY, David John , FROHN, Michael J. , CHEN, Ning , CHEN, Jian Jeffrey , SIEGMUND, Aaron C. , AMEGADZIE, Albert , TAMAYO, Nuria A. , BOOKER, Shon , GOODMAN, Clifford , WALTON, Mary , NISHIMURA, Nobuko , SHIN, Youngsook , LOW, Jonathan D. , CEE, Victor J. , REED, Anthony B. , WANG, Hui-Ling , LANMAN, Brian Alan
IPC分类号： C07D403/04 , C07D403/14 , C07D471/04 , C07D487/04 , A61P35/00 , A61K31/519
摘要： Provided herein are KRAS G12C inhibitors, composition of the same, and methods of using the same. These inhibitors are useful for treating a number of disorders, including pancreatic, colorectal, and lung cancers.

7. 发明申请

WO2019046150A1 MACROCYCLIC COMPOUNDS THAT INHIBIT MCL-1 PROTEIN 审中-公开
公开(公告)号：WO2019046150A1
公开(公告)日：2019-03-07
申请号：PCT/US2018/048058
申请日：2018-08-27
申请人： AMGEN INC.
发明人： BROWN, Sean P. , HARRINGTON, Paul E. , LANMAN, Brian Alan , LI, Kexue , LI, Yunxiao , LOW, Jonathan D. , MA, Vu Van , MINATTI, Ana Elena
IPC分类号： C07D513/08 , A61K31/554 , A61P35/00
CPC分类号： C07D513/08
摘要： Provided herein are myeloid cell leukemia 1 protein (Mcl-1) inhibitors, methods of their preparation, related pharmaceutical compositions, and methods of using the same. For example, provided herein are compounds of Formula I, or a stereoisomer thereof; and pharmaceutically acceptable salts thereof and pharmaceutical compositions containing the compounds. The compounds and compositions provided herein may be used, for example, in the treatment of diseases or conditions, such as cancer.

8. 发明申请

WO2022093856A1 HETEROCYCLIC SPIRO COMPOUNDS AND METHODS OF USE 审中-公开
公开(公告)号：WO2022093856A1
公开(公告)日：2022-05-05
申请号：PCT/US2021/056702
申请日：2021-10-26
申请人： AMGEN INC.
发明人： LANMAN, Brian Alan , BANERJEE, Abhisek , CHU-MOYER, Margaret , DAI, Dongcheng , KALLER, Matthew R. , LOPEZ, Patricia , MA, Vu Van , MANONI, Francesco , MEDINA, Jose M. , PICKRELL, Alexander J. , TAMAYO, Nuria A. , ZHU, Kai
IPC分类号： A61P35/00 , C07D487/10 , C07D491/04 , C07D513/04 , A61K31/506 , A61K31/519 , A61K31/541 , A61K31/517 , A61K31/5395
摘要： The present disclosure provides compounds of Formula (I) having activity as inhibitors of G12C mutant KRAS protein. This disclosure also provides pharmaceutical compositions comprising the compounds, uses and methods of treating certain disorders, such as cancer, including but not limited to lung, pancreatic and colorectal cancers.

9. 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).

10. 发明申请

WO2020050890A3 KRAS G12C INHIBITORS ENCOMPASSING A PIPERAZINE RING AND USE THEREOF IN THE TREATMENT OF CANCER 审中-公开
公开(公告)号：WO2020050890A3
公开(公告)日：2020-03-12
申请号：PCT/US2019/036626
申请日：2019-06-11
申请人： AMGEN INC.
发明人： ALLEN, John Gordon , LANMAN, Brian Alan , CHEN, Jian , REED, Anthony B. , CEE, Victor J. , LIU, Longbin , LOPEZ, Patricia , WURZ, Ryan Paul , NGUYEN, Thomas T. , BOOKER, Shon , ALLEN, Jennifer Rebecca , CHU-MOYER, Margaret , AMEGADZIE, Albert , CHEN, Ning , GOODMAN, Clifford , LOW, Jonathan D. , MA, Vu Van , MINATTI, Ana Elena , NISHIMURA, Nobuko , PICKRELL, Alexander J. , WANG, Hui-Ling , SHIN, Youngsook , SIEGMUND, Aaron C. , YANG, Kevin C. , TAMAYO, Nuria A. , WALTON, Mary , XUE, Qiufen
IPC分类号： C07D471/04 , C07D487/04 , A61K31/519 , A61K31/551 , A61P35/00 , A61K45/06
摘要： Provided herein are KRAS G12C inhibitors, such as [Insert Compound Here] composition of the same, and methods of using the same. These inhibitors are useful for treating a number of disorders, including pancreatic, colorectal, and lung cancers.

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