公开(公告)号：WO2021081212A1

公开(公告)日：2021-04-29

申请号：PCT/US2020/056874

申请日：2020-10-22

Applicant: AMGEN INC.

Inventor： WANG, Hui-Ling ,  CEE, Victor J.

IPC: C07D471/04 ,  C07D519/00 ,  A61P35/00 ,  A61K31/519

Abstract: Provided herein are KRAS G12C and KRAS G12D 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.

公开(公告)号：WO2020050890A2

公开(公告)日：2020-03-12

申请号：PCT/US2019/036626

申请日：2019-06-11

Applicant: AMGEN INC.

Inventor： 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

Abstract: 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.

公开(公告)号：WO2012148775A1

公开(公告)日：2012-11-01

申请号：PCT/US2012/034272

申请日：2012-04-19

Applicant: AMGEN INC. ,  D'AMICO, Derin C. ,  HERBERICH, Bradley J. ,  JACKSON, Claire L.M. ,  PETTUS, Liping H. ,  TASKER, Andrew ,  WANG, Hui-Ling ,  WU, Bin ,  WURZ, Ryan

Inventor： D'AMICO, Derin C. ,  HERBERICH, Bradley J. ,  JACKSON, Claire L.M. ,  PETTUS, Liping H. ,  TASKER, Andrew ,  WANG, Hui-Ling ,  WU, Bin ,  WURZ, Ryan

IPC: C07D487/04 ,  A61K31/495 ,  A61P35/00

CPC classification number: C07D487/04

Abstract: The invention relates to bicyclic compounds of formulas I and I', and salts thereof. In some embodiments, the invention relates to inhibitors or modulators of Pim-1 and/or Pim-2, and/or Pim-3 protein kinase activity or enzyme function. In still further embodiments, the invention relates to pharmaceutical compositions comprising compounds disclosed herein, and their use in the prevention and treatment of Pim kinase related conditions and diseases, preferably cancer.

Abstract translation: 本发明涉及式I和I'的双环化合物及其盐。 在一些实施方案中，本发明涉及Pim-1和/或Pim-2和/或Pim-3蛋白激酶活性或酶功能的抑制剂或调节剂。 在进一步的实施方案中，本发明涉及包含本文公开的化合物的药物组合物及其在预防和治疗Pim激酶相关病症和疾病，优选癌症中的用途。

公开(公告)号：WO2012078777A1

公开(公告)日：2012-06-14

申请号：PCT/US2011/063776

申请日：2011-12-07

Applicant: AMGEN INC. ,  WANG, Hui-Ling ,  BISWAS, Kaustav ,  CEE, Victor J. ,  CHAVEZ JR., Frank ,  HERBERICH, Bradley ,  JACKSON, Claire L.M. ,  LEE, Matthew ,  NIXEY, Thomas ,  PETTUS, Liping H. ,  REED, Anthony B. ,  RZASA, Robert M. ,  RUMFELT, Shannon ,  TASKER, Andrew ,  WU, Bin ,  WURZ, Ryan

Inventor： WANG, Hui-Ling ,  BISWAS, Kaustav ,  CEE, Victor J. ,  CHAVEZ JR., Frank ,  HERBERICH, Bradley ,  JACKSON, Claire L.M. ,  LEE, Matthew ,  NIXEY, Thomas ,  PETTUS, Liping H. ,  REED, Anthony B. ,  RZASA, Robert M. ,  RUMFELT, Shannon ,  TASKER, Andrew ,  WU, Bin ,  WURZ, Ryan

IPC: C07D401/14 ,  C07D403/04 ,  C07D403/14 ,  C07D405/14 ,  C07D413/14 ,  C07D417/14 ,  C07D471/04 ,  C07D487/04 ,  C07D498/04 ,  C07D491/107 ,  A61K31/497 ,  A61K31/437 ,  A61K31/506 ,  A61K31/444 ,  A61K31/4709

CPC classification number: C07D401/14 ,  C07D403/04 ,  C07D403/14 ,  C07D405/04 ,  C07D405/14 ,  C07D413/14 ,  C07D417/14 ,  C07D471/04

Abstract: The invention relates to bicyclic compounds of formula (1'), and salts thereof. In some embodiments, the invention relates to inhibitors or modulators of Pim-1 and/or Pim-2, and/or Pim-3 protein kinase activity or enzyme function. In still further embodiments, the invention relates to pharmaceutical compositions comprising compounds disclosed herein, and their use in the prevention and treatment of Pim kinase related conditions and diseases, preferably cancer.

Abstract translation: 本发明涉及式（1'）的双环化合物及其盐。 在一些实施方案中，本发明涉及Pim-1和/或Pim-2和/或Pim-3蛋白激酶活性或酶功能的抑制剂或调节剂。 在另外的实施方案中，本发明涉及包含本文公开的化合物的药物组合物及其在预防和治疗Pim激酶相关病症和疾病，优选癌症中的用途。

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

Applicant: AMGEN INC.

Inventor： 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: C07D403/04 ,  C07D403/14 ,  C07D471/04 ,  C07D487/04 ,  A61P35/00 ,  A61K31/519

Abstract: 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.

公开(公告)号：WO2019051291A1

公开(公告)日：2019-03-14

申请号：PCT/US2018/050044

申请日：2018-09-07

Applicant: AMGEN INC.

Inventor： LANMAN, Brian Alan ,  BOOKER, Shon ,  GOODMAN, Clifford ,  REED, Anthony B. ,  LOW, Jonathan D. ,  WANG, Hui-Ling ,  CHEN, Ning ,  MINATTI, Ana Elena ,  WURZ, Ryan ,  CEE, Victor J.

IPC: C07D471/04 ,  A61P35/00 ,  A61K31/519

Abstract: 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.

公开(公告)号：WO2004014871A1

公开(公告)日：2004-02-19

申请号：PCT/US2003/025191

申请日：2003-08-08

Applicant: AMGEN INC. ,  CHKRABARTI, Partha, P ,  CHEN, Ning ,  DOHERTY, Elisabeth, M. ,  DOMINGUEZ, Celia ,  FALSEY, James, Richard ,  FOTSH, Christopher, H. ,  HULME, Christopher ,  KATON, Jodie ,  NIXEY, Thomas ,  NORMAN, Mark, H. ,  OGNYANOV, Vassil, I. ,  PETTUS, Liping, H. ,  RZASA, Robert, Michael ,  STEC, Markian ,  WANG, Hui-Ling ,  ZHU, Jiawang

Inventor： CHKRABARTI, Partha, P ,  CHEN, Ning ,  DOHERTY, Elisabeth, M. ,  DOMINGUEZ, Celia ,  FALSEY, James, Richard ,  FOTSH, Christopher, H. ,  HULME, Christopher ,  KATON, Jodie ,  NIXEY, Thomas ,  NORMAN, Mark, H. ,  OGNYANOV, Vassil, I. ,  PETTUS, Liping, H. ,  RZASA, Robert, Michael ,  STEC, Markian ,  WANG, Hui-Ling ,  ZHU, Jiawang

IPC: C07D239/34

CPC classification number: C07D231/40 ,  C07D209/08 ,  C07D209/12 ,  C07D209/42 ,  C07D209/48 ,  C07D213/26 ,  C07D213/643 ,  C07D213/74 ,  C07D213/75 ,  C07D215/227 ,  C07D215/38 ,  C07D217/04 ,  C07D231/56 ,  C07D233/38 ,  C07D239/42 ,  C07D239/90 ,  C07D241/42 ,  C07D263/56 ,  C07D265/36 ,  C07D277/62 ,  C07D277/82 ,  C07D307/79 ,  C07D319/20 ,  C07D401/12 ,  C07D403/12 ,  C07D405/12 ,  C07D407/12 ,  C07D409/14 ,  C07D413/12 ,  C07D417/12

Abstract: 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.

Abstract translation: 具有通用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，牙齿疼痛，一般性头痛，偏头痛，丛集性头痛，混合血管和非血管性综合征，张力 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，具有炎性成分的皮肤病，慢性炎症，炎性疼痛和相关的痛觉过敏和异常性疼痛，神经性疼痛和相关 痛觉过敏和异常性疼痛，糖尿病性神经病疼痛，灼痛，交感神经维持性疼痛，传入神经缺失综合征，哮喘，上皮组织损伤或功能障碍，单纯疱疹，呼吸系统，泌尿生殖系统，胃肠或血管区域内脏运动障碍，伤口， 瘙痒症，白癜风，一般胃肠道 l溃疡，胃溃疡，十二指肠溃疡，腹泻，由坏死物质诱导的胃损伤，毛发生长，血管舒缩或过敏性鼻炎，支气管疾病或膀胱疾病。

公开(公告)号：WO2003101985A1

公开(公告)日：2003-12-11

申请号：PCT/US2003/016941

申请日：2003-05-29

Applicant: AMGEN INC. ,  HUANG, Qi ,  KALLER, Matthew ,  NGUYEN, Thomas ,  NORMAN, Mark, H. ,  RZASA, Robert ,  WANG, Hui-Ling ,  ZHONG, Wenge

Inventor： HUANG, Qi ,  KALLER, Matthew ,  NGUYEN, Thomas ,  NORMAN, Mark, H. ,  RZASA, Robert ,  WANG, Hui-Ling ,  ZHONG, Wenge

IPC: C07D417/14

CPC classification number: C07D417/14 ,  C07D403/04 ,  C07D409/14 ,  C07D417/04 ,  C07D471/04 ,  C07D491/04 ,  C07D513/04

Abstract: Compounds of formula (I) are effective for treatment of cell proliferation or apoptosis mediated diseases. The invention encompasses novel compounds and pharmaceutically acceptable derivatives thereof, pharmaceutical compositions and methods for prophylaxis and treatment of diseases and other maladies or conditions involving stroke, cancer and the like. The subject invention also relates to processes for making such compounds as well as to intermediates useful in such processes. Formula (I)

Abstract translation: 式（I）化合物对于治疗细胞增殖或凋亡介导的疾病是有效的。 本发明包括新颖的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中风，癌症等的病症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。

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

Applicant: AMGEN INC.

Inventor： 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: C07D471/04 ,  A61K31/4355 ,  A61K31/437 ,  A61K31/501 ,  A61P35/00 ,  C07D491/048 ,  C07D491/147 ,  C07D471/14 ,  C07D498/04 ,  C07D401/14 ,  C07D401/12 ,  C07D495/04

Abstract: 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).

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

Applicant: AMGEN INC.

Inventor： 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: C07D471/04 ,  C07D487/04 ,  A61K31/519 ,  A61K31/551 ,  A61P35/00 ,  A61K45/06

Abstract: 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.