CAS: 702-82-9; 3-Aminoadamantan-1-Ol

相似化合物

6240-03-5 42501-53-1 1382839-19-1

上下游产品

CAS号665-66-7 盐酸金刚烷胺 | CAS号67496-92-8 1-nitro-3-adama... | CAS号768-94-5 金刚烷胺 | CAS号274901-16-5 维达列汀 | CAS号1036959-23-5 维格列汀杂质2 | CAS号778-10-9 3-乙酰氨基-1-金刚烷醇

金刚烷胺置于硝化酸混合物,尿素,Potassium Hydroxide体系中,用97 %的收率获得产物3-胺基-1-金刚烷醇
参考文献:两亲性金刚烷衍生物的合成,红外和核磁共振强度:羟基化,乙酰化和氯化的影响
标题:两亲性金刚烷衍生物的合成,红外和核磁共振强度:羟基化,乙酰化和氯化的影响
摘要:新型氯代金刚酰胺被设计为具有更好的超分子位点,并通过羟基化,乙酰化和氯化合成.由于氯原子的特定电子特性,它赋予了更好的应用.在较温和的反应条件下,实现了高度惰性的金刚烷的官能化,总产率为 80%.以尿素为催化剂(10Mol%)进行金刚胺的羟基化,收率97%.使用酰化试剂(乙酰氯,1.1当量)和dipea(1.5当量)优化乙酰化,产率达到97%.最后,用亚硫酰氯(2.0当量)在65oc下进行氯化(产率84%).对所有产品的 Ir 和 NMR(包括 Do 交换)光谱以及 Esi-Ms 数据进行了分析.使用 B3Lyp 水平 {6-311++ (D,P) 基础设定}对所有产品进行 Dft 研究,以预测稳定性,反应性和其他全局描述符.
DOI:10.1016/j.Molstruc.2024.139265

专利信息

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: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-8937184-B2
优先权日:2005-02-16
标 题:1H-imidazole derivatives as cannabinoid CB2 receptor modulators
发明人：LANGE JOSEPHUS H M; VAN STUIVENBERG HERMAN H; VAN VLIET BERNARD J
权利人:LANGE JOSEPHUS H M; VAN STUIVENBERG HERMAN H; VAN VLIET BERNARD J; ABBVIE BV
摘要:The invention relates to a group of 1H-imidazole derivatives which are modulators of cannabinoid CB 2 receptors, to methods for the preparation of these compounds, to novel intermediates useful for the synthesis of said imidazole derivatives, to methods for the preparation of these intermediates, to pharmaceutical compositions containing one or more of these 1H-imidazole derivatives as active ingredient, as well as to the use of these pharmaceutical compositions for the treatment of disorders in which cannabinoid CB 2 receptors are involved. n The compounds have the general formula (I) n nwherein R 1 -R 4 have the meanings given in the specification.

专利号:US-2025049736-A1
优先权日:2021-12-16
标 题 :Sulfonamide derivatives and their use as soluble epoxide hydrolase inhibitors
发明人：IYER MALLIGA R; KUNDU BISWAJIT
权利人:THE US SECRETARY DEPARTMENT OF HEALTH
摘要:The present invention relates to compounds of formulae I and II. The compounds are useful for treating hypertension, atherosclerosis, pulmonary diseases, diabetes, pain, fibrosis, addictive disorders, inflammation, and immunological disorders or a condition treatable or preventable by inhibition of soluble epoxide hydrolase. Preferred compounds are N-((adamantan-1-yl)carbamoyl)-benzenesulfonamide derivatives. Exemplary compounds are e.g. •N—(((1r,3s,5R,7S)-3-hydroxyadamantan-1-yl)carbamoyl)-4-methylbenzenesulfonamide (example 14, compound 4a) •4-(tert-butyl)-N—(((1r,3s,5R,7S)-3-hydroxyadamantan-1-yl)carbamoyl)benzenesulfonamide (example 15, compound 4b) •N—(((1r,3s,5R,7S)-3-hydroxyadamantan-1-yl)carbamoyl)-4-(trifluoromethyl)benzenesulfonamide (example 16, compound 4j). The present description discloses the synthesis and characterisation of exemplary compounds as well as pharmacological data thereof.

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.