专利号:US-2024383853-A1 优先权日:2021-09-28 标题:Oximes and their use in treatment of gba-related diseases 发明人:NEVE SØREN; BROWN WILLIAM DALBY; THIRSTRUP KENNETH 权利人:ZEVRA DENMARK AS 摘要:The present invention relates to oximes, their synthesis, and their use for increasing GBA activity and/or levels as well as treatment of GBA-related diseases, such as Parkinson's disease.
专利号:US-8476313-B2 优先权日:2004-08-26 标 题:Heteroaryl-containing isoflavones as aromatase inhibitors 发明人:BRUEGGEMEIER ROBERT W; KIM YOUNG-WOO; HACKETT JOHN C 权利人:BRUEGGEMEIER ROBERT W; KIM YOUNG-WOO; HACKETT JOHN C; UNIV OHIO STATE RES FOUND 摘要:Compounds and methods useful for treating and prevention of cancer, particularly hormone-dependent breast cancer. Provided are compounds of formula I: n nwherein X is selected from O, N, S, SO, SO 2 , and S(CH 2 ) n , wherein n=1-10; R 1 and R 2 may be the same or different and are selected from H, OH, OCH 3 , OCH 2 CH 3 , OCH 2 C 6 H 5 , NH 2 , NHCH 3 , N(CH 3 ) 2 , CH 3 , CH 2 CH 3 , CH 2 CH 2 CH 3 , CH(CH 3 ) 2 , C(CH 3 ) 3 , NO 2 , F, Cl, Br, CF 3 , SH, SCH 3 , SCH 2 CH 3 , OCOCH 3 , OCOC(CH 3 ) 3 , OCOCH 2 COOH, and CN; and R 3 is a nitrogen-containing heterocyclic ring. Also provided are method for treating or preventing cancer in a subject by administering a therapeutically effective amount of a heteroaryl-containing isoflavone, or a pharmaceutically acceptable salt or prodrug thereof, to a subject in need of treatment. Also provided is a method for the synthesis of 2-substituted isoflavones by first reacting deoxybenzoins with a phase transfer catalyst to provide a 2-(alkylthio)isoflavone; second deprotecting the 2-(alkylthio)isoflavone; and third applying selective debenzylation to form the final compound.
专利号:US-2009209554-A1 优先权日:2004-03-24 标题 :Thiazoliums as transketolase inhibitors 发明人:BOYD STEVEN A; CONDROSKI KEVIN R; DE MEESE JASON; GONZALES STEPHEN S; GUNAWARDANA INDRANI W; KAPLAN TOMAS; HUEROU YVAN LE; LYSSIKATOS JOSEPH; ROMOFF TODD T; SULLIVAN FRANCIS X; THOMAS ALLEN 权利人:ARRAY BIOPHARMA INC 摘要:The present invention provides N-3′-pyridyl-methyl or N-2′-pyrazinylmethyl thiazolium derivatives of formula (I) which are useful as transketolase inhibitors wherein R 1 , R 2 , R 3 , Y, R 5 -R 9 , R a -R d , n and X − are as defined herein. The present invention also provides pharmaceutical compositions comprising the compounds of formula (I). The invention provides methods for inhibiting transketolase activity, reducing cellular ribose-5-phosphate levels, inhibiting nucleic acid synthesis, inhibiting cell proliferation and tumor cell growth in vitro and in vivo, stimulating apoptosis in tumor cells and treating cancer by administering a compound of formula (I) or a pharmaceutical composition thereof.
专利号:RU-2194701-C2 优先权日:1995-12-18 标 题 :Derivatives of quinazoline, methods of their synthesis, pharmaceutical composition comprising thereof and method of achievement of anti-angiogenic effect and/or effect of decrease of vascular penetration with their using