CAS: 16153-81-4; 4-(4-Methylpiperazin-1-yl)Phenylamine

相似化合物

170911-92-9 193902-64-6 125819-00-3

上下游产品

CAS号16155-03-6 1-甲基-4-(4-硝基苯基)哌嗪 | CAS号350-46-9 对氟硝基苯 | CAS号109-01-3 N-甲基哌嗪 | CAS号586-78-7 对溴硝基苯 | CAS号100-00-5 对硝基氯苯 | CAS号636-98-6 4-硝基碘苯 | CAS号144653-43-0 N-[4-(4-methylp... | CAS号23861-85-0 1-(4-异硫代氰酰基苯基)-... | CAS号955365-80-7 Adavosertib (MK... | CAS号1214265-56-1 WZ 3146 | CAS号1144072-40-1 1-[4-(4-Methyl-... | CAS号80259-18-3 JP 1302二盐酸盐 | CAS号879896-39-6 1-(4-异氰基苯基)-4-甲基哌嗪 | CAS号936092-52-3 5-甲基-N2-[4-(4-甲...

在 盐酸体系中,用 四氢呋喃,水 用作溶剂,以0.14 G的收率获得4-(4-甲基哌嗪)苯胺
参考文献:催化剂导向的溴-氯(杂)芳烃化学选择性双胺化反应:合成高级氨基苯胺中间体的合成路线
标题:催化剂导向的溴-氯(杂)芳烃化学选择性双胺化反应:合成高级氨基苯胺中间体的合成路线
摘要:开发了一种化学选择性顺序一锅偶联方案,以高产率制备几种氨基苯胺,作为活性药物成分(api)的组成部分.位点(亲电试剂上的cl对br)和亲核试剂(胺对亚胺)的选择性由所用催化剂决定.Pd-巴豆基(t-Buxphos)预催化剂即使在存在仲胺的情况下也选择性地将聚卤代芳烃的ar-Br与二苯甲酮亚胺偶联,而pd基的ruphos或(binap)pd(烯丙基)cl偶联ar-Cl位带有仲胺.
Doi:10.1021/acs.Orglett.8B00646

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-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.

专利号:EP-3904354-A1
优先权日:2020-04-30
标 题:New imidazolone derivatives as inhibitors of protein kinases in particular dyrk1a, clk1 and/or clk4
权利人:PERHA PHARMACEUTICALS
摘要:The present invention relates to a compound of formula (I)n nwherein R 1 represents a (C 1 -C 6 )alkyl group, a spiro(C 5 -C 11 )bicyclic ring, a fused phenyl group, a substituted phenyl group, a R'-L- group, wherein L is either a single bond or a (Ci-C3)alkanediyl group, and R' represents a (C 3 -C 8 )cycloalkyl group, a bridged (C6-C 10 )cycloalkyl group, a (C 3 -C 8 )heterocycloalkyl group, or a (C 3 -C 8 )heteroaryl group, or a R'-L- group wherein L is a (Ci-C3)alkanediyl group, and R' is a an optionally substituted phenyl group or any of its pharmaceutically acceptable salt. n 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. n 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; diabetes; regulation of folate and methionine metabolism; osteoarthritis; Duchenne muscular dystrophy; several cancers; neuroinflammation, anemia and infections and for regulating body temperature.

专利号:US-7615634-B2
优先权日:2003-02-10
标题:4-aminopyrimidine-5-one derivatives
发明人：BARTKOVITZ DAVID JOSEPH; CHU XIN-JIE; DING QINGJIE; JIANG NAN; LOVEY ALLEN JOHN; MOLITERNI JOHN ANTHONY; MULLIN JR JOHN GUILFOYLE; VU BINH THANH; WOVKULICH PETER MICHAEL
权利人:HOFFMANN LA ROCHE
摘要:Novel intermediate compounds are disclosed. These compounds are useful in the synthesis of 4-aminopyrimidine-5-one derivatives that inhibit cyclin-dependent kinases, in particular cyclin-dependent kinase 4 (Cdk4). The 4-aminopyrimidine-5-one derivatives and their pharmaceutically acceptable salts have antiproliferative activity and are useful in the treatment or control of cancer, in particular solid tumors.