专利号:US-10005720-B2 优先权日:2013-04-05 标题:Compounds useful for the treatment of metabolic disorders and synthesis of the same 发明人:SEXTON JONATHAN Z; BRENMAN JAY E; MUSSO DAVID L 权利人:NORTH CAROLINA CENTRAL UNIV; UNIV NORTH CAROLINA CHAPEL HILL 摘要:The present invention provides compounds of Formula (I): wherein variables X, Y, Z and R1 are as described herein. Some of the compounds described herein are glutamate dehydrogenase activators. The invention is also directed to pharmaceutical compositions comprising these compounds, uses of these compounds and compositions in the treatment of metabolic disorders as well as synthesis of the compounds.
专利号:US-9662347-B2 优先权日:2010-05-11 标题 :Method for inhibiting the induction of cell death by inhibiting the synthesis or secretion of age-albumin in cells of the mononuclear phagocyte system 发明人:LEE BONG HEE; BYUN KYUNG HEE 权利人:LEE BONG HEE; BYUN KYUNG HEE; GACHON UNIV OF INDUSTRY-ACADEMIC COOP FOUND 摘要:The present invention relates to a method for inhibiting the induction of cell death by inhibiting the synthesis or secretion of AGE-albumin in cells of the mononuclear phagocyte system, to an AGE-albumin synthesis inhibitor, and to a pharmaceutical composition comprising the AGE-albumin synthesis inhibitor for preventing or treating degenerative disease and autoimmune disease. The AGE-albumin of the present invention is synthesized and secreted in human microglia or human macrophages in an Alzheimer's model, stroke model, Parkinson's disease model and rheumatoid arthritis model. The AGE-albumin synthesis and secretion are caused by oxidative stress. The expression of RAGE increases in first-order human neurons or cartilage cells to which AGE-albumin is administered, whereupon a MAPK signaling pathway is activated and the expression of Bax increases to induce an increase in calcium in mitochondria, thus finally inducing cell death. Therefore, the AGE-albumin synthesis inhibitor of the present invention can be valuably used in the diagnosis or treatment of degenerative diseases or autoimmune diseases such as Alzheimer's disease, strokes, Parkinson's disease, amyotrophic lateral sclerosis, rheumatoid arthritis, diabetic retinopathy, AIDS, aging, pulmonary fibrosis, spinal cord injuries, etc.
专利号:US-4286098-A 优先权日:1980-03-28 标 题:Process for the preparation of chiral hydantoins 发明人:SARGES REINHARD 权利人:PFIZER 摘要:A novel process for the synthesis of chiral hydantoins of the structure ##STR1## wherein X is fluoro or chloro, from the corresponding 6-halo-4-chromanone of the structure ##STR2## is described. The compounds I are valuable in the treatment of certain chronic complications arising from diabetes mellitus. In addition the compound of the formula I wherein X is chloro possesses complementary hypoglycemic activity. n The process comprises the sequence of dehydrative coupling of the halochromanone (II) with S-(-)-alpha-methylbenzylamine to form the imine of structure ##STR3## addition of hydrogen cyanide to form the nitrile of structure ##STR4## condensation with chlorosulfonylisocyanate (or its equivalent) to form the alpha-methylbenzylhydantoin of structure ##STR5## and finally solvolysis of the latter to the chiral hydantoin of structure I.
专利号:US-4348526-A 优先权日:1980-03-28 标题:Intermediates in the preparation of chiral hydantoins 发明人:SARGES REINHARD 权利人:PFIZER 摘要:A novel process for the synthesis of chiral hydantoins of the structure ##STR1## wherein X is fluoro or chloro, from the corresponding 6-halo-4-chromanone of the structure ##STR2## is described. The compounds I are valuable in the treatment of certain chronic complications arising from diabetes mellitus. In addition the compound of the formula I wherein X is chloro possesses complementary hypoglycemic activity. n The process comprises the sequence of dehydrative coupling of the halochromanone (II) with S-(-)-alpha-methylbenzylamine to form the imine of structure ##STR3## addition of hydrogen cyanide to form the nitrile of structure ##STR4## condensation with chlorosulfonylisocyanate (or its equivalent) to form the alpha-methylbenzylhydantoin of structure ##STR5## and finally solvolysis of the latter to the chiral hydantoin of structure I.
专利号:US-2004267028-A1 优先权日:2001-09-24 标题 :Preparation and use of pyrrole derivatives for treating obesity 发明人:SMITH ROGER A; KLUENDER HAROLD C; SU NING; LAVOIE RICO C; FAN JIANMEI 权利人:SMITH ROGER A; KLUENDER HAROLD C; SU NING; LAVOIE RICO C; FAN JIANMEI 摘要:This invention relates to pyrrole derivatives which have been found to suppress appetite and induce weight loss. The invention also provides methods for synthesis of the compounds, pharmaceutical compositions comprising the compounds, and methods of using such compositions for inducing weight loss and treating obesity and obesity-related disorders.
专利号:US-2025223262-A1 优先权日:2022-03-31 标 题 :Synthesis of morphinans with reduced herg activity and mop binding 发明人:LAMMERT ECKHARD; SCHOLZ OKKA; OTTER SILKE; HEREBIAN DIRAN; HOFFMANN TORSTEN; SANZ MIGUEL ANGEL; KRAMP LAURENZ; LEVY LAURA MARIANA; HRISTEVA STANIMIRA 权利人:HEINRICH HEINE UNIV DUESSELDORF; DEUTSCHE DIABETES FORSCHUNGSGESELLSCHAFT E V; TAROS CHEMICALS GMBH & CO KG 摘要:The invention relates to morphinan-derivatives, processes for their preparation, medicaments containing them and the use of these morphinan-derivatives for the preparation of medicaments.
1: Aldawsari H, Altaf A, Banjar ZM, Iohara D, Nakabayashi M, Anraku M, Uekama K, Hirayama F. Crystallization of a new polymorph of acetohexamide from 2-hydroxybutyl-β-cyclodextrin solution: form VI with a high aqueous solubility. Int J Pharm. 2013 Sep 10;453(2):315-21. doi: 10.1016/j.ijpharm.2013.06.026. Epub 2013 Jun 21. doi: 10.1038/bjc.2012.580. Epub 2013 Jan 8. 3: Joseph KS, Anguizola J, Jackson AJ, Hage DS. Chromatographic analysis of acetohexamide binding to glycated human serum albumin. J Chromatogr B Analyt Technol Biomed Life Sci. 2010 Oct 15;878(28):2775-81. doi: 10.1016/j.jchromb.2010.08.021. Epub 2010 Aug 21. 4: Tokunaga H, Uchino T. [Studies for analyzing the prohibited ingredients such as acetohexamide in cosmetics]. Kokuritsu Iyakuhin Shokuhin Eisei Kenkyusho Hokoku. 2005;(123):19-22. Japanese. Epub 2001 Dec 20. Japanese.
合成参考文献
摘要:Drugs in Japan, 6(18), 1982 摘要:Drugs in Japan, -(34), 1995 摘要:TAKAGISHI Y ET AL; HIGH PERFORMANCE LIQUID CHROMATOGRAPHIC DETERMINATION OF ACETOHEXAMIDE & ITS METABOLITE HYDROXYHEXAMIDE; YAKUGAKU ZASSHI 99 (SEP) 961 (1979) 摘要:Ellenhorn, M.J., S. Schonwald, G. Ordog, J. Wasserberger. Ellenhorn's Medical Toxicology: Diagnosis and Treatment of Human Poisoning. 2nd ed. Baltimore, MD: Williams and Wilkins, 1997., p. 722 摘要:American Medical Association, AMA Department of Drugs, AMA Drug Evaluations. 3rd ed. Littleton, Massachusetts: PSG Publishing Co., Inc., 1977., p. 593