专利号:US-8153806-B2 优先权日:2000-11-30 标题:Synthesis of 4-amino-thalidomide enantiomers 发明人:TRESTON ANTHONY; SHAH JAMSHED H; D AMATO ROBERT J; HUNSUCKER KIMBERLY A; ROUGAS JOHN; CONNER BARRY P; PRIBDULA VICTOR; SWARTZ GLENN M 权利人:TRESTON ANTHONY; SHAH JAMSHED H; D AMATO ROBERT J; HUNSUCKER KIMBERLY A; ROUGAS JOHN; CONNER BARRY P; PRIBDULA VICTOR; SWARTZ GLENN M; CHILDRENS MEDICAL CENTER 摘要:The invention provides new and useful analogs of 4-amino-thalidomide. These analogs include S(−)-4-amino-thalidomide and R(+)-4-amino-thalidomide. The invention also provides processes for making these analogs. Further, the invention provides methods for inhibiting angiogenesis and treating angiogenesis-associated diseases, including cancer and macular degeneration, by administering these compounds.
专利号:US-2004147558-A1 优先权日:2000-11-30 标 题:Synthesis of 3-amino-thalidomide and its enantiomers
专利号:US-9669015-B2 优先权日:2005-04-07 标题 :Piperidine-2, 6-dione derivatives and their use as tumor necrosis factor inhibitors 发明人:ZHANG HESHENG 权利人:TIANJIN HEMAY BIO-TECH CO LTD 摘要:This invention is directed to derivatives of piperidine-2,6-dione, or their organic or inorganic salts thereof, a methods of synthesis of these derivatives, and their application as active pharmaceutical ingredient as inhibitors of TNFα releasing in cells, the derivative of piperidine-2,6-dione being of the general formula (I): n nwherein n represents 1, 2, 3, 4, 5 or 6; R 1 represents from one to four of the same or different substituents selected from F, Cl, Br, C 1-4 alkyl, OH, OC 1-4 alkyl, NO 2 , NHC(O)C 1-4 alkyl, NH 2 , NH(C 1-4 alkyl), N(C 1-4 alkyl) 2 ; R 2 represents OR 3 , NR 3 R 4 , N(R 3 )COR 4 , O 2 CR 5 ; R 3 and R 4 represent independently and at each occurrence H or C 1-4 alkyl; R 5 represents CHR 6 NR 7 R 8 , CHR 6 NR 9 C(O)CHR 10 NR 7 R 8 , a heterocycle W or CHR 6 NR 9 C(O)W; R 6 , R 9 , R 10 represent independently and at each occurrence H, or C 1-4 alkyl; R 7 and R 8 represent independently and at each occurrence H, C 1-4 alkyl, or R 7 and R 8 taken together represent 1,3-propylene, 1,4-butylene, 1,5-pentylene, or 1,6-hexylene; W represents four-membered, five-membered, six-membered, seven-membered, or eight-membered saturated or unsaturated heterocycle.
专利号:CA-2430669-C 优先权日:2000-11-30 标题 :Synthesis of 3-amino-thalidomide and its enantiomers
专利号:US-7812169-B2 优先权日:2000-11-30 标 题 :Method of synthesis of 4-amino-thalidomide enantiomers
专利号:AU-2002253795-B2 优先权日:2000-11-30 标 题:Synthesis of 4-Amino-Thalidomide enantiomers