-
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
Applicant: AMGEN INC.
Inventor: 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: C07K14/435
CPC classification number: C07K14/43518 , A61K38/00 , A61K38/1767 , A61K47/48284 , A61K47/48438 , A61K47/643 , A61K47/6817
Abstract: 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.
Abstract translation: 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。
-
2.VANILLOID RECEPTOR LIGANDS AND THEIR USE IN TREATMENTS 审中-公开
Title translation: VANILLOID受体配体及其在治疗中的应用公开(公告)号:WO2006113769A1
公开(公告)日:2006-10-26
申请号:PCT/US2006/014666
申请日:2006-04-17
Applicant: AMGEN INC.
Inventor: DOHERTY, Elizabeth M. , LIAO, Hongyu , NORMAN, Mark H. , RETZ, Daniel Martin
IPC: C07D401/14 , C07D403/12 , C07D417/14 , A61K31/506 , A61P29/00
CPC classification number: C07D417/14 , C07D401/14 , C07D403/12
Abstract: Compounds having the general structure ( formula (I)) 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: 具有一般结构的化合物(式(I))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,炎性肠病,炎症性眼病,炎症性或不稳定性膀胱病,牛皮癣,皮肤炎症成分炎症,慢性炎性病症,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,以及 异常性疼痛,糖尿病性神经病疼痛,灼痛,交感神经保持性疼痛,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,胃肠道或血管区域,伤口,烧伤,过敏性皮肤反应,瘙痒, 白癜风,一般胃肠炎 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。
-
公开(公告)号:WO2008153947A3
公开(公告)日:2008-12-18
申请号:PCT/US2008/007132
申请日:2008-06-05
Applicant: AMGEN INC. , SMITH, Adrian L. , DOHERTY, Elizabeth M. , HUANG, Qi , LIU, Gang
Inventor: SMITH, Adrian L. , DOHERTY, Elizabeth M. , HUANG, Qi , LIU, Gang
IPC: C07D473/00 , C07D487/04 , A61K31/519 , A61K31/52 , A61P35/00
Abstract: The present invention comprises a new class of compounds capable of modulating the activity of Raf kinase and, accordingly, useful for treatment of Raf kinase mediated diseases, including melanomas, tumors and other cancer-related conditions. The compounds have a general Formula (I) wherein each of A 1 , A 2 , A 3 , A 4 , A 5 , A 6 , A 7 , A 8 , A 9 , bond B, X, rings Z 1 and Z 2 , R 1 and R 3 are defined herein. The invention further comprises pharmaceutical compositions, methods for treatment of Raf kinase mediated diseases, and intermediates and processes useful for the preparation of compounds of the invention.
-
4.VANILLOID RECEPTOR LIGANDS AND THEIR USE IN TREATMENTS 审中-公开
Title translation: VANILLOID受体配体及其在治疗中的应用公开(公告)号:WO2006116563A1
公开(公告)日:2006-11-02
申请号:PCT/US2006/015947
申请日:2006-04-25
Applicant: AMGEN INC.
Inventor: DOHERTY, Elizabeth M. , KATON, Jodie , NORMAN, Mark H. , RETZ, Daniel Martin , WANG, Xianghong , BO, Yunxin Y. , TAMAYO, Nuria , NISHIMURA, Nobuko , LIAO, Hongyu
IPC: C07D239/42 , C07D401/04 , C07D401/14 , C07D403/04 , C07D413/04 , C07D403/12 , C07D213/74 , C07D401/10 , A61P29/00 , A61K31/505 , A61K31/506 , A61K31/5377 , A61K31/451
CPC classification number: C07D413/04 , C07D213/74 , C07D239/42 , C07D239/48 , C07D401/04 , C07D403/12 , C07D405/14
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。
-
公开(公告)号:WO2014099984A1
公开(公告)日:2014-06-26
申请号:PCT/US2013/075773
申请日:2013-12-17
Applicant: AMGEN INC.
Inventor: HOLDER, Jerry Ryan , SWAMINATH, Gayathri , MIRANDA, Leslie P. , ARAL, Jennifer , DOHERTY, Elizabeth M. , NIXEY, Thomas
CPC classification number: A61K47/48215 , A61K38/08 , A61K38/10 , A61K47/48415 , A61K47/60 , A61K47/6811 , C07K7/08 , C07K14/47 , C07K14/503
Abstract: The application is directed to APJ receptor agonist analogs having increased stability relative to the wild type apelin-13 and methods of using the agonist analogs. The analogs can be used, inter alia , in cardiac disorders such as heart failure.
Abstract translation: 该应用涉及相对于野生型apelin-13具有增加的稳定性的APJ受体激动剂类似物和使用激动剂类似物的方法。 类似物尤其可用于心脏病,例如心力衰竭。
-
6.PYRIMIDINE DERIVATIVES FOR USE AS VANILLOID RECEPTOR LIGANDS AND THEIR USE IN THE TREATMENT OF PAIN 审中-公开
Title translation: 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
Applicant: AMGEN INC.
Inventor: WANG, Hui-Ling , BALAN, Chenera , DOHERTY, Elizabeth M. , FALSEY, James R. , GORE, Vijay Keshav , KATON, Jodie , NORMAN, Mark H.
IPC: C07D417/12
CPC classification number: C07D401/12 , C07D403/12 , C07D405/12 , C07D413/12 , C07D417/12 , C07D417/14 , C07D471/04
Abstract: 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.
Abstract translation: 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。
-
7.VANILLOID RECEPTOR LIGANDS AND THEIR USE IN TREATMENTS 审中-公开
Title translation: VANILLOID受体配体及其在治疗中的应用公开(公告)号:WO2005077938A1
公开(公告)日:2005-08-25
申请号:PCT/US2005/004370
申请日:2005-02-11
Applicant: AMGEN INC.
Inventor: BALAN, Chenera , CHEN, Ning , DOHERTY, Elizabeth M. , GORE, Vijay Keshav , NORMAN, Mark H. , WANG, Hui-Ling
IPC: C07D401/12
CPC classification number: C07D401/12 , C07D401/14 , C07D403/12 , C07D403/14 , C07D413/12 , C07D417/12 , C07D417/14
Abstract: Compounds having the general structure (I) 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 syndroms, 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(I)的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 胃肠道疾病 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。
-
公开(公告)号:EP2170887A2
公开(公告)日:2010-04-07
申请号:EP08768206.8
申请日:2008-06-05
Applicant: Amgen Inc.
Inventor: SMITH, Adrian L. , DOHERTY, Elizabeth M. , HUANG, Qi , LIU, Gang
IPC: C07D473/00 , C07D487/04 , A61K31/519 , A61K31/52 , A61P35/00
CPC classification number: C07D487/04 , C07D473/00
Abstract: The present invention comprises a new class of compounds capable of modulating the activity of Raf kinase and, accordingly, useful for treatment of Raf kinase mediated diseases, including melanomas, tumors and other cancer-related conditions. The compounds have a general Formula (I) wherein each of A1, A2, A3, A4, A5, A6, A7, A8, A9, bond B, X, rings Z1 and Z2, R1 and R3 are defined herein. The invention further comprises pharmaceutical compositions, methods for treatment of Raf kinase mediated diseases, and intermediates and processes useful for the preparation of compounds of the invention.
-
9.VANILLOID RECEPTOR LIGANDS AND THEIR USE IN TREATMENTS 审中-公开
Title translation: VANILLOIDREZEPTORLIGANDEN和它们在疗程组合公开(公告)号:EP1883632A1
公开(公告)日:2008-02-06
申请号:EP06751590.8
申请日:2006-04-25
Applicant: Amgen Inc.
Inventor: DOHERTY, Elizabeth M. , KATON, Jodie , NORMAN, Mark H. , RETZ, Daniel Martin , WANG, Xianghong , BO, Yunxin Y. , TAMAYO, Nuria , NISHIMURA, Nobuko , LIAO, Hongyu
IPC: C07D239/42 , C07D401/04 , C07D401/14 , C07D403/04 , C07D413/04 , C07D403/12 , C07D213/74 , C07D401/10 , A61P29/00 , A61K31/505 , A61K31/506 , A61K31/5377 , A61K31/451
CPC classification number: C07D413/04 , C07D213/74 , C07D239/42 , C07D239/48 , C07D401/04 , C07D403/12 , C07D405/14
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.
-
10.VANILLOID RECEPTOR LIGANDS AND THEIR USE IN TREATMENTS 审中-公开
Title translation: VANILLOIDREZEPTORLIGANDEN和它们在疗程组合公开(公告)号:EP1745034A1
公开(公告)日:2007-01-24
申请号:EP05722957.7
申请日:2005-02-11
Applicant: AMGEN INC.
Inventor: BALAN, Chenera , CHEN, Ning , DOHERTY, Elizabeth M. , GORE, Vijay Keshav , NORMAN, Mark H. , WANG, Hui-Ling
IPC: C07D401/12 , C07D417/12 , C07D413/12 , C07D403/12 , C07D417/14 , C07D401/14 , C07D403/14 , A61K31/44 , A61K31/444
CPC classification number: C07D401/12 , C07D401/14 , C07D403/12 , C07D403/14 , C07D413/12 , C07D417/12 , C07D417/14
Abstract: Compounds having the general structure (I) 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 syndroms, 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.
-
-
-
-
-
-
-
-
-