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CAS号67528-24-9 (1S,2S)-2-bromo... | CAS号438051-03-7 tert-butyl N-[(... | CAS号768-22-9 6,6A-二氢-1AH-茚并[... | CAS号7480-35-5 顺式-1-氨基-2,3-二氢-... | CAS号95-13-6 茚 | CAS号180681-90-7 (1S,2R)-2-bromo... | CAS号7480-35-5 顺式-1-氨基-2,3-二氢-... | CAS号438051-03-7 tert-butyl N-[(...📜(2-羟基-2,3-二氢-1H-茚-1-基)氨基甲酸叔丁酯置于盐酸体系中,用 甲醇,水 用作溶剂,以100%的收率获得(1S,2S)-(+)-反式-1-氨基-2-茚醇
参考文献:探索配体设计中的结构多样性:氨基茚满醇案例
标题:探索配体设计中的结构多样性:氨基茚满醇案例
摘要:合成了一系列基于氨基茚满醇骨架的对映体纯配体,但在区域化学和立体化学上有所不同.这些配体已经被方便地衍生化,并且已经筛选了它们在不同对映选择性反应中的催化效率,从而为每个考虑的方法确定了关于区域化学和立体化学的优先候选者.氨基取代基的性质已针对特定应用进行了优化,这导致开发了一种通过还原胺化制备大体积双环胺的有效方法.
Doi:10.1002/adsc.200800420
专利信息
专利号:US-6960601-B2
优先权日:2001-09-24
标题 :Preparation and use of imidazole derivatives for treatment of obesity
发明人:SMITH ROGER A; O'CONNOR STEPHEN J; WIRTZ STEPHAN-NICHOLAS; WONG WAI C; CHOI SOONGYU; KLUENDER HAROLD C E; SU NING; WANG GAN; ACHEBE FURAHI; YING SHIHONG
权利人:BAYER PHARMACEUTICALS CORP
摘要:This invention relates to substituted imidazole 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:WO-2023072961-A1
优先权日:2021-10-26
标题:Imidazolone derivatives as inhibitors of protein kinases in particular dyrk1a, clk1 and/or clk4
发明人:DEAU EMMANUEL; GEORGE PASCAL; MEIJER LAURENT; MIEGE FRÉDÉRIC
权利人:PERHA PHARMACEUTICALS
摘要:The present invention relates to a compound of formula (I) wherein R 2 is selected from the group consisting of a hydrogen atom and a (C 1 -C 3 )alkyl group, R 3 is a (C 1 -C 4 )alkyl or a (C 3 -C 6 )cycloalkyl group, R 1 represents a (C 4 -C 6 )alkyl group, a (C 3 -C 8 )cycloalkyl group, a bridged (C 6 -C 10 )cycloalkyl group, a fused phenyl group, a substituted phenyl group, a R'-L- group, wherein L is either a single bond or a (C 1 -C 3 )alkanediyl group, and R' represents a (C 3 -C 8 )heterocycloalkyl group, or a (C 3 -C 8 )heteroaryl group, or a R''-L- group wherein L is a (C 1 -C 3 )alkanediyl group, and R'' is a an optionally substituted phenyl group or any of its pharmaceutically acceptable salt. The present invention further relates to a composition comprising a compound of formula (I) and a process for manufacturing said compound as well as its synthesis intermediates. It also relates to said compound for use as a medicament, in particular in the treatment and/or prevention of cognitive deficits and neuroinflammation associated with Down syndrome; Alzheimer's disease; dementia; tauopathies; Parkinson's disease; CDKL5 Deficiency Disorder; Phelan-McDermid syndrome; autism; type 1 and type 2 diabetes; abnormal folate and methionine metabolism; tendinopathy and osteoarthritis; Duchenne muscular dystrophy; cancers and leukemias; neuroinflammation, anemia, infections caused by unicellular parasites, viral infections and for regulating body temperature.
专利号:WO-2023072966-A1
优先权日:2021-10-26
标题:Imidazolone derivatives as inhibitors of protein kinases in particular dyrk1a, clk1 and/or clk4
发明人:DEAU EMMANUEL; GEORGE PASCAL; MEIJER LAURENT; MIEGE FRÉDÉRIC
权利人:PERHA PHARMACEUTICALS
摘要:The present invention relates to a compound of formula (I) wherein R 1 represents a (C 4 -C 6) alkyl group, a (C 3 -C 8) cycloalkyl group, a bridged (C 6 -C 10 )cycloalkyl group, a fused phenyl group, a substituted phenyl group, a R'-L- group, wherein L is either a single bond or a (C 1 -C 3 )alkanediyl group, and R' represents, a (C 3 -C 8 )heterocycloalkyl group, or a (C 3 -C 8 )heteroaryl group, or a R''-L- group wherein L is a (C 1 -C 3 )alkanediyl group, and R'' is an optionally substituted phenyl group; R 2 is selected from the group consisting of a hydrogen atom and a (C 1 -C 3 )alkyl group; R 5 represents a hydrogen atom, a (C 1 -C 4 )alkyl group or a (C 3 -C 6 )cycloalkyl group or any of its pharmaceutically acceptable salt. The present invention further relates to a composition comprising a compound of formula (I) and a process for manufacturing said compound as well as its synthesis intermediates. It also relates to said compound for use as a medicament, in particular in the treatment and/or prevention of cognitive deficits and neuroinflammation associated with Down syndrome; Alzheimer's disease; dementia; tauopathies; Parkinson's disease; CDKL5 Deficiency Disorder; Phelan-McDermid syndrome; autism; type 1 and type 2 diabetes; abnormal folate and methionine metabolism; osteoarthritis and tendinopathy; Duchenne muscular dystrophy; cancers and leukemias; neuroinflammation, anemia, infections caused by unicellular parasites, viral infections and for regulating body temperature.
专利号:US-7220870-B2
优先权日:1995-03-14
标 题:Hydrolytic kinetic resolution of cyclic substrates
发明人:JACOBSEN ERIC N; TOKUNAGA MAKOTO; LARROW JAY F
权利人:HARVARD COLLEGE
摘要:The present invention relates to a process for stereoselective or regioselective chemical synthesis which generally comprises reacting a nucleophile and a chiral or prochiral cyclic substrate in the presence of a non-racemic, chiral catalyst to produce a stereoisomerically- and/or regioisomerically-enriched product. The present invention also relates to hydrolytic kinetic resolutions of racemic and diastereomeric mixtures of epoxides.
专利号:WO-2023072969-A1
优先权日:2021-10-26
标题 :Imidazolone derivatives as inhibitors of protein kinases in particular dyrk1a, clk1 and/or clk4
发明人:DEAU EMMANUEL; GEORGE PASCAL; MEIJER LAURENT; MIEGE FRÉDÉRIC; ARCHAMBAUD SYLVIE
权利人:PERHA PHARMACEUTICALS
摘要:The present invention relates to a compound of formula (I) wherein A, B, C, D and E are selected from the group consisting of =CH- and -N=, R 2 is selected from a hydrogen atom, a (C 1 -C 4 )alkyl group and a (C 3 -C 6 )cycloalkyl group, R 1 represents a (C 4 -C 6 )alkyl group, a (C 3 -C 8 )cycloalkyl group, a bridged (C 6 -C 10 )cycloalkyl group, a fused phenyl group, a substituted phenyl group, a R'-L- group, wherein L is either a single bond or a (C 1 -C 3 )alkanediyl group, and R' represents, a (C 3 -C 8 )heterocycloalkyl group, or a (C 3 -C 8 )heteroaryl group, or a R'-L- group wherein L is a (C 1 -C 3 )alkanediyl group, and R' is a an optionally substituted phenyl group or any of its pharmaceutically acceptable salt. The present invention further relates to a composition comprising a compound of formula (I) and a process for manufacturing said compound as well as its synthesis intermediates. It also relates to said compound for use as a medicament, in particular in the treatment and/or prevention of cognitive deficits and neuroinflammation associated with Down syndrome, Alzheimer's disease, dementia and/or tauopathies; Parkinson's disease; CDKL5 Deficiency Disorder; Phelan-McDermid syndrome; autism; type 1 and type 2 diabetes; abnormal folate and methionine metabolism; tendinopathy and osteoarthritis; Duchenne muscular dystrophy; several cancers; neuroinflammation, anemia, infections and for regulating body temperature.
专利号:US-12398129-B2
优先权日:2020-04-30
标 题 :Imidazolone derivatives as inhibitors of protein kinases in particular DYRK1A, CLK1 and/or CLK4
发明人:DEAU EMMANUEL; GEORGE PASCAL; MEIJER LAURENT; MIEGE FRÉDÉRIC
权利人:PERHA PHARMACEUTICALS
摘要:The present invention relates to a compound of formula (I) wherein R1 represents a (C1-C6)alkyl group, a spiro(C5-C11)bicyclic ring, a fused phenyl group, a substituted phenyl group, a R′-L- group, wherein L is either a single bond or a (C1-C3)alkanediyl group, and R′ represents a (C3-C8)cycloalkyl group, abridged (C6-C10)cycloalkyl group, a (C3-C8)heterocycloalkyl group, or a (C3-C8)heteroaryl group, or a R′-L- group wherein L is a (C1-C3)alkanediyl group, and R′ is an optionally substituted phenyl group, and wherein R2 represents a hydrogen atom or a (C1-C3)alkyl group or any of its pharmaceutically acceptable salt. The present invention further relates to a composition comprising a compound of formula (I) and a process for manufacturing said compound as well as its synthesis intermediates. It also relates to said compound for use as a medicament, in particular in the treatment and/or prevention of cognitive deficits associated with Down syndrome; Alzheimer's disease; dementia; tauopathies; Parkinson's disease; CDKL5 Deficiency Disorder; Phelan-McDermid syndrome; autism; type 1 and type 2 diabetes; abnormal folate and methionine metabolism; osteoarthritis; Duchenne muscular dystrophy; several cancers; neuroinflammation, anemia and viral and unicellular infections and for regulating body temperature.