专利号:WO-2007056417-A3 优先权日:2005-11-07 标题 :Synthesis of alendronate sodium trihydrate 发明人:O'CEALLAIGH TOMAS 权利人:MERCK & CO INC; O'CEALLAIGH TOMAS 摘要:This invention describes a process for the synthesis of alendronate sodium trihydrate from the reaction of alendronic acid, either anhydrous or in a hydrated state, in an aqueous slurry with sodium hydroxide in water. The pH is adjusted into the range 4.3 - 4.4, the solution is concentrated and the sodium salt thus formed is isolated by crystallization from water.
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:EP-1494680-B1 优先权日:2002-03-25 标题 :Use of carbon-2-modified-vitamin d analogs to induce the formation of new bone 发明人:DELUCA HECTOR F; PIKE J WESLEY; SHEVDE NIRUPAMA K 权利人:WISCONSIN ALUMNI RES FOUND 摘要:It has been discovered that the 2-carbon-modified derivatives of 1α,25-dihydroxyvitamin D3 specifically stimulate osteoblasts to form new bone. The ability of the 2-carbon-modified vitamin D analogs to stimulate new bone formation suggest that these compounds can be used where synthesis of new bone is required. Thus, these compounds can be used either systemically or locally to stimulate the growth of bone transplants, to increase the rate of fracture healing and thereby reduce the time required for the healing of fractures, the stimulation of bone growth when required for replacement surgery, and also for the growth of bone to implants or other devices required to maintain the skeleton or teeth in the proper positions.
专利号:US-7956214-B2 优先权日:2001-11-02 标题 :Process for the preparation of aniline-derived thyroid receptor ligands 发明人:CHIDAMBARAM RAMAKRISHNAN; KANT JOYDEEP; WEAVER RAYMOND E; YU JURONG; GHOSH ARUN 权利人:KAROBIO AB; BRISTOL MYERS SQUIBB CO 摘要:Provided are processes for the synthesis of aniline derivatives, specifically certain aniline derivatives which have activity as thyroid receptor ligands.
专利号:US-8815883-B2 优先权日:2009-11-02 标 题 :Compounds and methods for inhibiting serotonin synthesis 发明人:LANDRY DONALD; DENG SHI-XIAN 权利人:LANDRY DONALD; DENG SHI-XIAN; TRUSTEES OF COLUMBIA UNVIERSITY IN THE CITY OF NEW YORK 摘要:Compounds having the structures below that are TPH1 inhibitors are provided: The compounds are useful of, e.g., to increase bone mass. In preferred embodiments, the patient is known to have, or to be at risk for, a low bone mass disease such as osteoporosis.
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.
1: Imai K. Alendronate sodium hydrate (oral jelly) for the treatment of osteoporosis: review of a novel, easy to swallow formulation. Clin Interv Aging. 2013;8:681-8. doi: 10.2147/CIA.S37199. Epub 2013 Jun 7. Review. 2: Ananchenko G, Novakovic J, Tikhomirova A. Alendronate sodium. Profiles Drug Subst Excip Relat Methodol. 2013;38:1-33. doi: 10.1016/B978-0-12-407691-4.00001-0. Review. Review. German. Review. Review. Chinese. doi: 10.1007/s10067-012-2060-y. Epub 2012 Aug 30. Review. doi: 10.1111/j.1742-1241.2011.02806.x. Epub 2012 Feb 7. Review. doi: 10.1016/j.jconrel.2011.11.037. Epub 2011 Dec 8. Review. doi: 10.1016/j.joms.2011.03.046. Epub 2011 Aug 4. Review. doi: 10.1007/s00774-011-0281-9. Epub 2011 Jun 14. Review.
合成参考文献
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