专利号:US-2025206743-A1 优先权日:2022-03-25 标 题:Tyk2 inhibitor synthesis and intermediates thereof 发明人:MASSE CRAIG E; PHADKE AVINASH S; LAWSON JON P; LEVY STUART; YANG XIAOWEI; WU GUISHENG; FAN SHUFENG 权利人:TAKEDA PHARMACEUTICALS CO 摘要:Described herein are methods of synthesis of a tyrosine-protein kinase 2 (TYK2) inhibitor and to intermediate compounds of the synthesis and methods of making the intermediates. Also provided are pharmaceutically acceptable compositions including compounds prepared by the synthetic method and methods of treating disorders using the same.
专利号:US-2007155693-A1 优先权日:2004-01-19 标 题 :Inhibitor of cancer bone metastasis 发明人:YAGITA AKIKUNI 权利人:ORIENT CANCER THERAPY CO LTD 摘要:The subject of the present invention is to provide means to fully achieve the inhibition of cancer bone metastasis, which was accomplished through the repeated selection of agents with aiming at obtaining more beneficial effects on the inhibition of cancer bone metastasis. The invention is achieved by combining an inhibition substance of the activation of osteoclast caused by the degradation of a signaling molecule, TRAF6, in the activation of osteoclast, a suppressive substance of the differentiation from osteoclast precursor cells to mature osteoclasts, and/or a bone resorption inhibitor and/or a Cox2 synthesis inhibitor. This combination was found to have an extremely high utility for the inhibition of cancer bone metastasis. Further, the invention is achieved by the inhibitor of cancer bone metastasis, wherein an IL-12 production inducer as an inhibition substance of the activation of osteoclast caused by the degradation of a signaling molecule, TRAF6, in the activation of osteoclast, a tyrosine kinase inhibitor as a suppressive substance of the differentiation from osteoclast precursor cells to mature osteoclasts, and/or a bisphosphonate as a bone resorption inhibitor and/or a Cox2 synthesis inhibitor for inhibiting the stimulation of RANKL/RANK receptor are combined.
专利号:US-11993606-B2 优先权日:2015-10-16 标题:Processes for the preparation of (3S,4R)-3-ethyl-4-(3H-imidazo[1,2-a]pyrrolo[2,3-e]-pyrazin-8-yl)-n-(2,2,2-trifluoroethyl)pyrrolidine-1-carboxamide and solid state forms thereof 发明人:MOHAMED MOHAMED-ESLAM F; OTHMAN AHMED A; PANGAN AILEEN L; SONG IN-HO; KLÜNDER BEN; VOSS JEFFREY W; PADLEY ROBERT J; CAMP HEIDI S 权利人:ABBVIE INC 摘要:The present disclosure relates to processes for preparing (3S,4R)-3-ethyl-4-(3H-imidazo[1,2-a]pyrrolo[2,3-e]pyrazin-8-yl)-N-(2,2,2-trifluoroethyl)pyrrolidine-1-carboxamide, solid state forms thereof, and corresponding pharmaceutical compositions, methods of treatment (including treatment of rheumatoid arthritis and various spondyloarthritic conditions, including types of axial spondyloarthritis (axSpA)), kits, methods of synthesis, and products-by-process. In various aspects, provided are methods for treating active non-radiographic axSpA (nr-axSpA) and methods for treating active ankylosing spondylitis (AS).
专利号:US-11976077-B2 优先权日:2015-10-16 标 题 :Processes for the preparation of (3S,4R)-3-ethyl-4-(3H-imidazo[1,2-α]pyrrolo[2,3-e]-pyrazin-8-yl)-n-(2,2,2-trifluoroethyl)pyrrolidine-1-carboxamide and solid state forms therof 发明人:PANGAN AILEEN L; TEIXEIRA HENRIQUE D; MOHAMED MOHAMED-ESLAM F; OTHMAN AHMED A; KLÜNDER BEN; VOSS JEFFREY W; PADLEY ROBERT J; CAMP HEIDI S 权利人:ABBVIE INC 摘要:The present disclosure relates to processes for preparing (3S,4R)-3-ethyl-4-(3H-imidazo[1,2-a]pyrrolo[2,3-e]pyrazin-8-yl)-N-(2,2,2-trifluoroethyl)pyrrolidine-1-carboxamide, solid state forms thereof, and corresponding pharmaceutical compositions, methods of treatment (including treatment of rheumatoid arthritis and atopic dermatitis), kits, methods of synthesis, and products-by-process.
专利号:US-11512092-B2 优先权日:2015-10-16 标题 :Processes for the preparation of (3S,4R)-3-ethyl-4-(3H-imidazo[1,2-a]pyrrolo[2,3-e]-pyrazin-8-yl)-n-(2,2,2-trifluoroethyl)pyrrolidine-1-carboxamide and solid state forms thereof 发明人:ALLIAN AYMAN; JAYANTH JAYANTHY; MOHAMED MOHAMED-ESLAM F; MULHERN MATHEW; NORDSTROM FREDRIK LARS; OTHMAN AHMED A; ROZEMA MICHAEL J; BHAGAVATULA LAKSHMI; MARROUM PATRICK J; MAYER PETER T; SHEIKH AHMAD Y; BORCHARDT THOMAS B; KLÜNDER BEN 权利人:ABBVIE INC 摘要:The present disclosure relates to processes for preparing (3S,4R)-3-ethyl-4-(3H-imidazo[1,2-a]pyrrolo[2,3-e]pyrazin-8-yl)-N-(2,2,2-trifluoroethyl)pyrrolidine-1-carboxamide, solid state forms thereof, and corresponding pharmaceutical compositions, methods of treatment (including treatment of rheumatoid arthritis and various spondyloarthritic conditions, including types of axial spondyloarthritis (axSpA)), kits, methods of synthesis, and products-by-process. In various aspects, provided are methods for treating active non-radiographic axSpA (nr-axSpA) and methods for treating active ankylosing spondylitis (AS).
专利号:US-11524964-B2 优先权日:2015-10-16 标题:Processes for the preparation of (3S,4R)-3-ethyl-4-(3H-imidazo[1,2-a]pyrrolo[2,3-e]-pyrazin-8-yl)-n-(2,2,2-trifluoroethyl)pyrrolidine-1-carboxamide and solid state forms thereof 发明人:MOHAMED MOHAMED-ESLAM F; OTHMAN AHMED A; KLÜNDER BEN; PANGAN AILEEN L; SONG IN-HO 权利人:ABBVIE INC 摘要:The present disclosure relates to processes for preparing (3S,4R)-3-ethyl-4-(3H-imidazo[1,2-a]pyrrolo[2,3-e]pyrazin-8-yl)-N-(2,2,2-trifluoroethyl)pyrrolidine-1-carboxamide, solid state forms thereof, and corresponding pharmaceutical compositions, methods of treatment (including treatment of rheumatoid arthritis and various spondyloarthritic conditions, including types of axial spondyloarthritis (axSpA)), kits, methods of synthesis, and products-by-process. In various aspects, provided are methods for treating active non-radiographic axSpA (nr-axSpA) and methods for treating active ankylosing spondylitis (AS).
1: Quesada-Gómez JM, Santiago-Mora R, Navarro-Valverde C, Dorado G, Casado-Díaz A. Stimulation of in-vitro angiogenesis by low concentrations of risedronate is mitigated by 1,25-dihydroxyvitamin D3 or 24,25-dihydroxyvitamin D3. J Steroid Biochem Mol Biol. 2015 Apr;148:214-8. doi: 10.1016/j.jsbmb.2014.10.018. Epub 2014 Nov 1. Review. Review. 3: Hemmati I, Wade J, Kelsall J. Risedronate-associated scleritis: a case report and review of the literature. Clin Rheumatol. 2012 Sep;31(9):1403-5. doi: 10.1007/s10067-012-2035-z. Epub 2012 Aug 5. Review. Review. Erratum in: Med Lett Drugs Ther. 2011 Jun 27;53(1367):52. doi: 10.3349/ymj.2010.51.2.164. Epub 2010 Feb 12. Review. 6: Epstein S, Jeglitsch M, McCloskey E. Update on monthly oral bisphosphonate therapy for the treatment of osteoporosis: focus on ibandronate 150 mg and risedronate 150 mg. Curr Med Res Opin. 2009 Dec;25(12):2951-60. doi: 10.1185/03007990903361307. Review. Review. Japanese. doi: CliCa081014171426. Review. Japanese. doi: 10.1002/14651858.CD004523.pub3. Review. Review. Japanese. Review.