专利号:US-8178712-B2 优先权日:2006-06-23 标 题:Process for the synthesis of Ibandronate sodium 发明人:RAO DHARAMARAJ RAMCHANDRA; KANKAN RAJENDRA NARAYANRAO; GHAGARE MARUTI GANPATI 权利人:RAO DHARAMARAJ RAMCHANDRA; KANKAN RAJENDRA NARAYANRAO; GHAGARE MARUTI GANPATI; CIPLA LTD 摘要:The present invention relates to an improved process for the synthesis of Ibandronate sodium of formula (I). The present invention also provides novel processes for the synthesis of 3-[N-(methylpentyl)amino]propionic acid (III).
专利号:US-12391691-B2 优先权日:2018-11-16 标题:Synthesis of key intermediate of KRAS G12C inhibitor compound 发明人:PARSONS ANDREW THOMAS; COCHRAN BRIAN MCNEIL; POWAZINIK IV WILLIAM; CAPORINI MARC ANTHONY 权利人:AMGEN INC 摘要:The present invention relates to an improved, efficient, scalable process to prepare intermediate compounds, such as compound 5M, having the structure n nuseful for the synthesis of compounds that target KRAS G12C mutations, such as
专利号:US-2025206736-A1 优先权日:2019-11-14 标题 :Synthesis of kras g12c inhibitor compound 发明人:CORBETT MICHAEL THOMAS; CAILLE SEBASTIEN 权利人:AMGEN INC 摘要:The present disclosure relates to an improved, efficient, scalable process to prepare intermediate compounds, such as 2-isopropyl-4-methylpyridin-3-amine, useful for the synthesis of compounds, such as Compound 9, for the treatment of KRAS G12C mutated cancers.
专利号:WO-2017100796-A1 优先权日:2015-12-11 标 题 :Modulation of globoseries glycosphingolipid synthesis and cancer biomarkers 发明人:WONG CHI-HUEY; HSU TSUI-LING; WU CHUNG-YI; CHEUNG SARAH K C; CHUANG PO-KAI 权利人:SINACA ACAD; WONG CHI-HUEY; HSU TSUI-LING 摘要:The present disclosure relates to methods and compositions which can modulate the globoseries glycosphingolipid synthesis. Particularly, the present disclosure is directed to glycoenzyme inhibitor compound and compositions and methods of use thereof that can modulate the synthesis of globoseries glycosphingolipid SSEA-3/SSEA-4/GloboH in the biosynthetic pathway; particularly, the glycoenzyme inhibitors target the alpha-4GalT; beta- 4GalNAcT-I; or beta-3GalT-V enzymes in the globoseries synthetic pathway. Additionally, the present disclosure is also directed to vaccines, antibodies, and/or immunogenic conjugate compositions targeting the SSEA-3/SSEA-4/GLOBO H associated epitopes (natural and modified) which elicit antibodies and/or binding fragment production useful for modulating the globoseries glycosphingolipid synthesis. Moreover, the present disclosure is also directed to the method of using the compositions described herein for the treatment or detection of hyperproliferative diseases and/or conditions. Furthermore, the instant disclosure also relates to cancer stem cell biomarkers for disgnostic and therapeutic uses.
专利号:EP-1566177-A1 优先权日:2004-02-23 标 题:The use of bisphosphonates for treating skin by stimulating of collagen synthesis 发明人:KIM JIN; YOOK JONG IN; KIM NAM HEE; RYU JU KYOUNG 权利人:TIGEN BIOTECH CO LTD 摘要:The present invention relates to a novel use of bisphosphonate, and morenparticularly to a composition for increasing collagen synthesis comprisingnbisphosphonate as an active ingredient, as well as the use thereof. The inventivencomposition comprising the bisphosphonate promotes collagen synthesis, and thus, whennit is applied to the skin, it reduces wrinkles of the skin and makes the skin elastic. Fornthis reason, the inventive composition will be useful as cosmetics for the prevention ornimprovement of skin aging or a wound-healing agent. Furthermore, the inventivencomposition can remarkably increase the collagen synthesis of fibroblasts in vitro , andnthus, can be effectively used in the production of products containing collagen.
专利号:US-2017283878-A1 优先权日:2015-12-11 标题:Modulation of globoseries glycosphingolipid synthesis and cancer biomarkers 发明人:WONG CHI-HUEY; WU CHUNG-YI; CHEUNG SARAH K C; CHUANG PO-KAI; HSU TSUI-LING 权利人:ACADEMIA SINICA 摘要:The present disclosure relates to methods and compositions which can modulate the globoseries glycosphingolipid synthesis. Particularly, the present disclosure is directed to glycoenzyme inhibitor compound and compositions and methods of use thereof that can modulate the synthesis of globoseries glycosphingolipid SSEA-3/SSEA-4/GloboH in the biosynthetic pathway; particularly, the glycoenzyme inhibitors target the alpha-4GalT; beta-4GalNAcT-I; or beta-3GalT-V enzymes in the globoseries synthetic pathway. Additionally, the present disclosure is also directed to vaccines, antibodies, and/or immunogenic conjugate compositions targeting the SSEA-3/SSEA-4/GLOBO H associated epitopes (natural and modified) which elicit antibodies and/or binding fragment production useful for modulating the globoseries glycosphingolipid synthesis. Moreover, the present disclosure is also directed to the method of using the compositions described herein for the treatment or detection of hyperproliferative diseases and/or conditions. Furthermore, the instant disclosure also relates to cancer stem cell biomarkers for diagnostic and therapeutic uses.
参考文献:10.4049/jimmunol.0903454 摘要:D'Asaro M, La Mendola C, Di Liberto D, Orlando V, Todaro M, Spina M, Guggino G, Meraviglia S, Caccamo N, Messina A, Salerno A, Di Raimondo F, Vigneri P, Stassi G, Fourniè JJ, Dieli F. V gamma 9V delta 2 T lymphocytes efficiently recognize and kill zoledronate-sensitized, imatinib-sensitive, and imatinib-resistant chronic myelogenous leukemia cells. J Immunol. 2010 Mar 15;184(6):3260–8. doi: 10.4049/jimmunol.0903454. 参考文献:10.1007/bf03327451 摘要:Verhaar HJJ. Medical treatment of osteoporosis in the elderly. Aging Clinical and Experimental Research. 2009 Dec;21(6):407–13. doi: 10.1007/bf03327451. 参考文献:10.1007/s11596-011-0111-7 摘要:Liu H, Chen A, Guo F, Yuan L. Influence of osteopontin short hairpin RNA on the proliferation and invasion of human renal cancer cells. J Huazhong Univ Sci Technolog Med Sci. 2010 Feb;30(1):61–8. doi: 10.1007/s11596-011-0111-7. 参考文献:10.1007/s11596-010-0121-5 摘要:Fang J, Zheng C, Tao H, Zhao H, Ren J, Feng G. Therapeutic effects of all trans-retinoic acid combined with transarterial chemoembolization on Walker-256 hepatoma in rats. J Huazhong Univ Sci Technolog Med Sci. 2010 Feb;30(1):113–8. doi: 10.1007/s11596-010-0121-5. 参考文献:10.1016/j.joms.2009.08.027 摘要:Oizumi T, Funayama H, Yamaguchi K, Yokoyama M, Takahashi H, Yamamoto M, Kuroishi T, Kumamoto H, Sasaki K, Kawamura H, Sugawara S, Endo Y. Inhibition of Necrotic Actions of Nitrogen-Containing Bisphosphonates (NBPs) and Their Elimination From Bone by Etidronate (a Non-NBP): A Proposal for Possible Utilization of Etidronate as a Substitution Drug for NBPs. Journal of Oral and Maxillofacial Surgery. 2010 May;68(5):1043–54. doi: 10.1016/j.joms.2009.08.027.