公开(公告)号：WO2009091374A2

公开(公告)日：2009-07-23

申请号：PCT/US2008/011724

申请日：2008-10-14

Applicant: AMGEN INC. ,  ALBRECHT, Brian K. ,  BAUER, David ,  BELLON, Steven ,  BODE, Christiane M. ,  BOOKER, Shon ,  BOEZIO, Alessandro ,  CHOQUETTE, Deborah ,  D'AMICO, Erin ,  HARMANGE, Jean-christophe ,  HIRAI, Satoko ,  HUNGATE, Randall W. ,  KIM, Tae-seong ,  LEWIS, Richard T. ,  LIU, Longbin ,  LOHMAN, Julia ,  NORMAN, Mark H. ,  POTASHMAN, Michelle ,  SIEGMUND, Aaron C. ,  SPRINGER, Stephanie ,  STEC, Markian ,  XI, Ning ,  YANG, Kevin ,  PETERSON, Emily, A. ,  ROMERO, Karina ,  COPELAND, Katrina, W.

Inventor： ALBRECHT, Brian K. ,  BAUER, David ,  BELLON, Steven ,  BODE, Christiane M. ,  BOOKER, Shon ,  BOEZIO, Alessandro ,  CHOQUETTE, Deborah ,  D'AMICO, Erin ,  HARMANGE, Jean-christophe ,  HIRAI, Satoko ,  HUNGATE, Randall W. ,  KIM, Tae-seong ,  LEWIS, Richard T. ,  LIU, Longbin ,  LOHMAN, Julia ,  NORMAN, Mark H. ,  POTASHMAN, Michelle ,  SIEGMUND, Aaron C. ,  SPRINGER, Stephanie ,  STEC, Markian ,  XI, Ning ,  YANG, Kevin ,  PETERSON, Emily, A. ,  ROMERO, Karina ,  COPELAND, Katrina, W.

IPC: C07D471/04 ,  C07D487/04 ,  C07D493/04 ,  C07D495/04 ,  C07D498/04 ,  A61K31/4355

CPC classification number: A61K31/538 ,  A61K31/437 ,  A61K31/497 ,  A61K31/5025 ,  A61K31/506 ,  A61K31/52 ,  A61K31/5377 ,  A61K45/06 ,  C07D403/12 ,  C07D471/04 ,  C07D473/34 ,  C07D487/04 ,  C07D493/04 ,  C07D495/04 ,  C07D498/04 ,  C07D519/00

Abstract: Selected compounds are effective for prophylaxis and treatment of diseases, such as HGF mediated diseases. 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, cancer and the like. The subject invention also relates to processes for making such compounds as well as to intermediates useful in such processes.

Abstract translation: 所选化合物对于预防和治疗诸如HGF介导的疾病等疾病是有效的。 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，用于预防和治疗疾病和其它疾病或涉及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：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：WO2022046690A1

公开(公告)日：2022-03-03

申请号：PCT/US2021/047237

申请日：2021-08-24

Applicant: AMGEN INC.

Inventor： HUCKLE, James E. ,  STEC, Markian ,  WU, Tian ,  REID, Darren L. ,  AVAREZ-NUNEZ, Fernando Antonio ,  BROWN, Sean P.

IPC: A61K9/14 ,  A61P35/00 ,  A61K31/553 ,  C07D519/00

Abstract: Provided herein are solid dispersions comprising AMG 397, methods of preparing the solid dispersion, and pharmaceutical formulations comprising AMG 397.

公开(公告)号：WO2003099284A1

公开(公告)日：2003-12-04

申请号：PCT/US2003/016655

申请日：2003-05-20

Applicant: AMGEN INC. ,  DOHERTY, Elizabeth, M. ,  ZHU, Jiawang ,  STEC, Markian ,  NORMAN, Mark, H. ,  KELLY, Michael, G. ,  FOTSCH, Christopher, H. ,  CHEN, Ning ,  CHAKRABARTI, Partha, P. ,  HUNGATE, Randy, W.

Inventor： DOHERTY, Elizabeth, M. ,  ZHU, Jiawang ,  STEC, Markian ,  NORMAN, Mark, H. ,  KELLY, Michael, G. ,  FOTSCH, Christopher, H. ,  CHEN, Ning ,  CHAKRABARTI, Partha, P. ,  HUNGATE, Randy, W.

IPC: A61K31/501

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 ,  C07D237/20 ,  C07D239/42 ,  C07D239/90 ,  C07D241/42 ,  C07D263/56 ,  C07D265/36 ,  C07D277/62 ,  C07D277/82 ,  C07D307/79 ,  C07D319/20 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D405/12 ,  C07D407/12 ,  C07D409/14 ,  C07D413/12 ,  C07D417/12 ,  C07D417/14 ,  C07D471/04

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, pruritis, 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，瘙痒症，白癜风，一般胃肠道疾病， 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。

公开(公告)号：WO2010132598A1

公开(公告)日：2010-11-18

申请号：PCT/US2010/034596

申请日：2010-05-12

Applicant: AMGEN INC. ,  BODE, Christiane ,  BOEZIO, Alessandro ,  CHENG, Alan, C. ,  CHOQUETTE, Deborah ,  COATS, James, R. ,  COPELAND, Katrina, W. ,  HUANG, Hongbing ,  LA, Daniel ,  LEWIS, Richard ,  LIAO, Hongyu ,  POTASHMAN, Michele ,  STELLWAGEN, John ,  YI, Shuyan ,  NORMAN, Mark ,  STEC, Markian ,  PETERSON, Emily, A. ,  GRACEFFA, Russell

Inventor： BODE, Christiane ,  BOEZIO, Alessandro ,  CHENG, Alan, C. ,  CHOQUETTE, Deborah ,  COATS, James, R. ,  COPELAND, Katrina, W. ,  HUANG, Hongbing ,  LA, Daniel ,  LEWIS, Richard ,  LIAO, Hongyu ,  POTASHMAN, Michele ,  STELLWAGEN, John ,  YI, Shuyan ,  NORMAN, Mark ,  STEC, Markian ,  PETERSON, Emily, A. ,  GRACEFFA, Russell

IPC: C07D401/14 ,  C07D403/04 ,  C07D403/14 ,  C07D471/04 ,  C07D487/04 ,  C07D519/00 ,  A61K31/506 ,  A61K31/437 ,  A61K31/52 ,  A61K31/53 ,  A61P35/00

CPC classification number: C07D401/14 ,  C07D403/04 ,  C07D403/14 ,  C07D471/04 ,  C07D487/04 ,  C07D519/00

Abstract: The present invention provides compounds that are PIKK inhibitors, more specifically, mTOR and/or PI3Kα kinase inhibitors and are therefore useful for the treatment of diseases treatable by inhibition of kinases, specifically PI3 kinases, more specifically, mTOR and/or PI3Kα, such as cancer. Also provided are pharmaceutical compositions containing such compounds and processes for preparing such compounds.

Abstract translation: 本发明提供了PIKK抑制剂，更具体地，mTOR和/或PI3Ka激酶抑制剂的化合物，因此可用于治疗通过抑制激酶可以治疗的疾病，特别是PI3激酶，更具体地，mTOR和/或PI3Kα，例如 癌症。 还提供含有这些化合物的药物组合物和制备这些化合物的方法。

公开(公告)号：WO2008008539A2

公开(公告)日：2008-01-17

申请号：PCT/US2007/016068

申请日：2007-07-13

Applicant: AMGEN INC. ,  ALBRECHT, Brian ,  BAUER, David ,  BELLON, Steven ,  BODE, Christiane ,  BOOKER, Shon ,  BOEZIO, Alessandro ,  CHOQUETTE, Deborah ,  D'AMICO, Derin ,  HARMANGE, Jean-Christophe ,  HIRAI, Satoko ,  HUNGATE, Randall ,  KIM, Tae-Seong ,  LEWIS, Richard ,  LIU, Longbin ,  LOHMAN, Julia ,  NORMAN, Mark ,  POTASHMAN, Michele ,  SIEGMUND, Aaron ,  SPRINGER, Stephanie ,  STEC, Markian ,  XI, Ning ,  YANG, Kevin

Inventor： ALBRECHT, Brian ,  BAUER, David ,  BELLON, Steven ,  BODE, Christiane ,  BOOKER, Shon ,  BOEZIO, Alessandro ,  CHOQUETTE, Deborah ,  D'AMICO, Derin ,  HARMANGE, Jean-Christophe ,  HIRAI, Satoko ,  HUNGATE, Randall ,  KIM, Tae-Seong ,  LEWIS, Richard ,  LIU, Longbin ,  LOHMAN, Julia ,  NORMAN, Mark ,  POTASHMAN, Michele ,  SIEGMUND, Aaron ,  SPRINGER, Stephanie ,  STEC, Markian ,  XI, Ning ,  YANG, Kevin

IPC: C07D471/04 ,  C07D473/34 ,  C07D487/04 ,  A61K31/5025 ,  A61K31/52 ,  A61K31/437 ,  A61P35/00

CPC classification number: C07D471/04

Abstract: Selected compounds are effective for prophylaxis and treatment of diseases, such as HGF mediated diseases. 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, cancer and the like. The subject invention also relates to processes for making such compounds as well as to intermediates useful in such processes.

Abstract translation: 所选化合物对于预防和治疗诸如HGF介导的疾病等疾病是有效的。 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，用于预防和治疗疾病和其它疾病或涉及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：WO2003009850A1

公开(公告)日：2003-02-06

申请号：PCT/US2002/023926

申请日：2002-07-25

Applicant: AMGEN INC.

Inventor： 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: A61K31/495

CPC classification number: 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

Abstract: 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.

Abstract translation: 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。

公开(公告)号：WO2002066470A1

公开(公告)日：2002-08-29

申请号：PCT/US2002/000743

申请日：2002-01-11

Applicant: AMGEN INC.

Inventor： CHEN, Guoqing ,  ADAMS, Jeffrey ,  BEMIS, Jean ,  BOOKER, Shon ,  CAI, Guolin ,  CROGHAN, Michael ,  DIPIETRO, Lucian ,  DOMINGUEZ, Celia ,  ELBAUM, Daniel ,  GERMAIN, Julie ,  GEUNS-MEYER, Stephanie ,  HANDLEY, Michael ,  HUANG, Qi ,  KIM, Joseph, L. ,  KIM, Tae-Seong ,  KISELYOV, Alexander ,  OUYANG, Xiaohu ,  PATEL, Vinod, F. ,  SMITH, Leon, M. ,  STEC, Markian ,  TASKER, Andrew ,  XI, Ning ,  XU, Shimin ,  YUAN, Chester, Chenguang

IPC: C07D409/12

CPC classification number: C07D213/82 ,  A61K31/443 ,  A61K31/4439 ,  A61K31/444 ,  A61K31/4545 ,  A61K31/4709 ,  A61K31/4725 ,  A61K31/496 ,  A61K31/506 ,  A61K31/5377 ,  A61K31/538 ,  C07D401/12 ,  C07D401/14 ,  C07D405/12 ,  C07D405/14 ,  C07D409/00 ,  C07D409/04 ,  C07D409/12 ,  C07D409/14 ,  C07D413/14 ,  C07D417/14 ,  C07D471/04

Abstract: Selected heterocyclic compounds are effective for prophylaxis and treatment of diseases, such as angiogenesis mediated diseases. The invention encompasses novel compounds, analogs, prodrugs and pharmaceutically acceptable derivatives thereof, pharmaceutical compositions and methods for prophylaxis and treatment of diseases and other maladies or conditions involving, cancer and the like. The subject invention also relates to processes for making such compounds as well as to intermediates useful in such processes.

Abstract translation: 所选择的杂环化合物对于预防和治疗诸如血管生成介导的疾病等疾病是有效的。 本发明包括新型化合物，类似物，前药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：WO2021202452A1

公开(公告)日：2021-10-07

申请号：PCT/US2021/024779

申请日：2021-03-30

Applicant: AMGEN INC.

Inventor： ACHMATOWICZ, Michael ,  CUI, Sheng ,  HWANG, Tsang-Lin ,  LANGILLE, Neil Fred ,  TOM, Janine K. ,  HUCKLE, James E. ,  STEC, Markian ,  WU, Tian ,  BROWN, Sean P.

IPC: C07D519/00 ,  A61P35/00 ,  A61K31/553

Abstract: Disclosed herein is an improved process for the synthesis of compound (A): (A), or a salt or solvate thereof via methylation of compound (B): (B), or a salt or solvate thereof, a crystalline hydrate of compound A, and pharmaceutical formulations comprising a crystalline hydrate of compound (A).

公开(公告)号：WO2009085230A1

公开(公告)日：2009-07-09

申请号：PCT/US2008/013940

申请日：2008-12-18

Applicant: AMGEN INC. ,  BOOKER, Shon ,  KIM, Tae-seong ,  LIAO, Hongyu ,  LIU, Longbin ,  NORMAN, Mark H. ,  PETERSON, Emily Anne ,  STEC, Markian ,  TAMAYO, Nuria A.

Inventor： BOOKER, Shon ,  KIM, Tae-seong ,  LIAO, Hongyu ,  LIU, Longbin ,  NORMAN, Mark H. ,  PETERSON, Emily Anne ,  STEC, Markian ,  TAMAYO, Nuria A.

IPC: C07D471/04 ,  C07D487/04 ,  A61K31/4162 ,  A61P35/00

CPC classification number: C07D471/04 ,  C07D487/04

Abstract: The present invention relates to compounds of Formula I, or a pharmaceutically acceptable salt thereof, that inhibit phosphoinositide 3-kinase; Formula (I) methods of treating diseases or conditions, such as cancer, using the compounds; and pharmaceutical compositions containing the compounds.

Abstract translation: 本发明涉及抑制磷酸肌醇3-激酶的式I化合物或其药学上可接受的盐; 式（I）使用该化合物治疗疾病或病症如癌症的方法; 和含有这些化合物的药物组合物。