专利号:US-9926291-B2 优先权日:2007-03-27 标 题 :Synthesis of thiohydantoins 发明人:OUERFELLI OUATHEK; DILHAS ANNA; YANG GUANGBIN; ZHAO HONG 权利人:SLOAN KETTERING INST CANCER RES 摘要:A novel synthesis of the anti-androgen, A52, which has been found to be useful in the treatment of prostate cancer, is provided. A52 as well as structurally related analogs may be prepared via the inventive route. This new synthetic scheme may be used to prepare kilogram scale quantities of pure A52.
专利号:EP-0946499-B1 优先权日:1996-11-22 标 题 :N-(aryl/heteroaryl/alkylacetyl) amino acid amides, pharmaceutical compositions comprising same, and methods for inhibiting beta-amyloid peptide release and/or its synthesis by use of such compounds 发明人:WU JING; TUNG JAY S; NISSEN JEFFREY S; MABRY THOMAS E; LATIMER LEE H; EID CLARK NORMAN; AUDIA JAMES E 权利人:ELAN PHARM INC; LILLY CO ELI 摘要:Disclosed are compounds which inhibit beta -amyloid peptide release and/or its synthesis, and, accordingly, have utility in treating Alzheimer's disease. Also disclosed are pharmaceutical compositions comprising a compound which inhibits beta -amyloid peptide release and/or its synthesis as well as methods for treating Alzheimer's disease both prophylactically and therapeutically with such pharmaceutical compositions. Said compounds are represented by formula (I), wherein R<1> is selected from the group consisting of: a) alkyl, alkenyl, alkaryl, alkcycloalkyl, aryl, cycloalkyl, cycloalkenyl, heteroaryl and heterocyclic; b) a substituted phenyl group of formula (II), wherein R is alkylene of from 1 to 8 carbon atoms, m is an integer equal to 0 or 1, and c) 1- or 2-naphthyl substituted at the 5, 6, 7 and/or 8 positions, R<2> is selected from the group consisting of hydrogen, alkyl of from 1 to 4 carbon atoms, alkylalkoxy of from 1 to 4 carbon atoms, alkylthioalkoxy of from 1 to 4 carbon atoms; and R<3> and R<3'> are independently selected from the group consisting of: (a) hydrogen, (b) alkyl, (c) -(R<7>)n(W)p, wherein R<7> is an alkylene group, W is selected from the group consisting of (i) formula (A); (ii) heteroaryl; and (iii) N-heterocyclic, and n is an integer equal to 0 or 1, and p is an integer equal to 1 to 3; (d) -CH( phi )CH2C(O)O-Q where Q is selected from the group consisting of alkyl, aryl, heteroaryl and heterocyclic; X' is hydrogen, hydroxy or fluoro; X'' is hydrogen, hydroxy or fluoro, or X' and X'' together form an oxo group, Z is selected from the group consisting of a bond covalently linking R<1> to -CX'X''-, oxygen and sulfur.
专利号:US-6262302-B1 优先权日:1996-11-22 标题:N-(aryl/heteroaryl/alkylacetyl) amino acid amides, pharmaceutical compositions comprising same, and methods for inhibiting β-amyloid peptide release and/or its synthesis by use of such compounds 发明人:WU JING; TUNG JAY S; NISSEN JEFFREY S; MABRY THOMAS E; LATIMER LEE H; EID CLARK N; AUDIA JAMES E 权利人:ELAN PHARM INC; LILLY CO ELI 摘要:Disclosed are compounds which inhibit beta-amyloid peptide release and/or its synthesis, and, accordingly, have utility in treating Alzheimer's disease. Also disclosed pharmaceutical compositions comprising a compound which inhibits beta-amyloid peptide release and/or its synthesis as well as methods for treating Alzheimer's disease both prophylactically and therapeutically with such pharmaceutical compositions.
专利号:WO-2008119015-A2 优先权日:2007-03-27 标 题 :Synthesis of thiohydantoins
专利号:US-8987452-B2 优先权日:2007-03-27 标 题:Synthesis of thiohydantoins
专利号:WO-9321213-A1 优先权日:1992-04-16 标题 :Alpha-aminoboronic acid peptides and their use as elastase inhibitors 发明人:BERNSTEIN PETER ROBERT; SHAW ANDREW; SHENVI ASHOKKUMAR BHIKKAPPA; THOMAS ROYSTON MARTIN; WARNER PETER; WOLANIN DONALD JOHN 权利人:ZENECA LTD 摘要:The present invention relates to certain novel heterocyclic derivatives which are 1-pyridylacetamide derivatives of formula (I), set out herein, which are inhibitors of human leukocyte elastase (HLE), also known as human neutrophil elastase (HNE), making them useful whenever such inhibition is desired, such as for research tools in pharmacological, diagnostic and related studies and in the treatment of diseases on mammals in which (HLE) is implicated. The invention also includes intermediates useful in the synthesis of these heterocyclic derivatives, processes for preparing the heterocyclic derivatives, pharmaceutical compositions containing such heterocyclic derivatives and methods for their use.
[参考文献]: Nanjing Zhang, Et Al. 5-Azidoepibatidine: An Exceptionally Potent Photoaffinity Ligand For Neuronal Alpha 4 Beta 2 And Alpha 7 Nicotinic Acetylcholine Receptors. Bioorg Med Chem Lett. 2003 Feb 10;13(3):525-7.
合成参考文献
摘要:Riva, R.; Banfi, L.; Basso, A., Science of Synthesis: Multicomponent Reactions, (2013) 1, 353. 摘要:c E. Spinner and G.B. Yeoh. J. Chem. Soc., B 1971, 296.