相似化合物
20010-99-5 39204-49-4 2227206-03-1欧盟法规
ECHA物质C&L通报上下游产品
5-methylpyrazine-2-carbonitrile 2,5-dimethyl-pyrazine 01179-7JAC01179-7 3-Bromo-4-(6-cyano-1-ethyl-1H-indazol-3-ylmethyl)-N-(5-methyl-pyrazin-2-ylmethyl)-benzamide 2-(4-Fluoro-phenoxy)-N-(5-methyl-pyrazin-2-ylmethyl)-nicotinamide 合成工艺路线路线简述
- 合成目标产物 2-(Aminomethyl)-5-Methylpyrazine 主要起始原料 2,5-Dimethyl Pyrazine
- 98006-91-8 = 132664-85-8
反应条件:1.1 Reagents: Hydrogen,Ammonia Catalysts: Nickel Solvents: Methanol; 24 H,35 Bar,80 °C
标题:Stable And Reusable Ni-Based Nanoparticles For General And Selective Hydrogenation Of Nitriles To Amines
作者:Ma,Zhuang; Chandrashekhar,Vishwas G.; Zhou,Bei; Alenad,Asma M.; Rockstroh,Nils; Et Al
参考文献:Chemical Science 日期:2022 卷标:13(36) 页码:10914-10922
📜2-甲基-5-氰基哌嗪置于氨,氢气体系中,用 甲醇 用作溶剂,80.0 °C,4.0 Mpa 条件下,反应 24.0H,以73%的收率获得2-氨甲基-5-甲基吡嗪
参考文献:稳定且可重复使用的镍基纳米颗粒,用于将腈类普遍和选择性氢化成胺
标题:稳定且可重复使用的镍基纳米颗粒,用于将腈类普遍和选择性氢化成胺
摘要:二氧化硅负载的超小 Ni 纳米颗粒允许在温和条件下将各种腈类普遍和选择性地氢化为伯胺.通过煅烧由 Ni( Ii ) 生成的模板材料)硝酸盐和胶体二氧化硅在空气下,随后在分子氢存在下还原,制备最佳催化剂.制备的负载型纳米颗粒稳定,使用方便,易于回收利用.最佳催化剂材料的适用性通过对超过 110 种不同的脂肪族和芳香族腈(包括功能化和工业相关底物)进行氢化来证明.具有挑战性的杂环腈,特别是氰基吡啶,以非常好的收率提供了相应的伯胺.所得胺可作为制备众多生命科学产品和聚合物的重要前体和中间体.
Doi:10.1039/d2Sc02961H
专利信息
专利号:US-7468375-B2
优先权日:2004-04-26
标题:Inhibitors of the HIV integrase enzyme
发明人:DRESS KLAUS RUPRECHT; HU QIYUE; JOHNSON TED WILLIAM; PLEWE MICHAEL BRUNO; TANIS STEVEN PAUL; WANG HAI; YANG ANLE; YIN CHUNFENG; ZHANG JUNHU
权利人:PFIZER
摘要:The present invention is directed to compounds of formula (I), and pharmaceutically acceptable salts and solvates thereof, their synthesis, and their use as modulators or inhibitors of the human immunodeficiency virus (“HIVâ€?) integrase enzyme.
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-2011124634-A1
优先权日:2008-05-13
标 题:Bioactive compounds for treatment of cancer and neurodegenerative diseases
发明人:SUN CONNIE L; LI XIAOYUAN
权利人:PONIARD PHARMACEUTICALS INC
摘要:The invention provides bioactive compounds for the treatment of various malconditions such as cancer and neurodegenerative diseases including Alzheimer's disease. The chemical compounds as disclosed herein are found to show bioactivity in bioassays related to these conditions. Pharmaceutical compositions, combinations and methods of synthesis are provided, as are methods of using the compound, compositions and combinations in the treatment of the diseases.
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-2022220095-A1
优先权日:2019-04-26
标 题 :N-((HETEROARYL)METHYL)-1-TOSYL-1H-PYRAZOLE-3-CARBOXAMIDE DERIVATIVES AS Kv3 POTASSIUM CHANNEL ACTIVATORS FOR TREATING NEUROLOGICAL AND PSYCHIATRIC DISORDERS
发明人:SAMS ANETTE GRAVEN; RASMUSSEN LARS KYHN; YU WANWAN
权利人:H LUNDBECK AS
摘要:The present invention provides N-(heteroaryl)methyl)-1-tosyl-1H-pyrazole-3-carboxamide derivatives of the structure Formula (I), which activate the Kv3 potassium channels. Separate aspects of the invention are directed to pharmaceutical compositions comprising said compounds and to the compounds and pharmaceutical compositions thereof for use in methods of medical treatment of disorders responsive to the activation of Kv3 potassium channels, such as e.g. neurological or psychiatric disorders for example epilepsy, schizophrenia, cognitive impairment associated with schizophrenia (CIAS), autism spectrum disorder, bipolar disorder, ADHD, anxiety-related disorders, depression, cognitive dysfunction, Alzheimer's disease, Fragile X syndrome, chronic pain, hearing loss, sleep and circadian disorders, and sleep disruption. Exemplary compounds are e.g.: •4-methyl-N-((5-methylpyrazin-2-yl)methyl)-1-tosyl-1H-pyrazole-3-carboxamide (example 1; compound 32), •N-((1-methyl-1H-pyrazol-4-yl)methyl)-1-tosyl-1H-pyrazole-3-carboxamide (example 2; compound 62) •1-((4-(difluoro methoxy)phenypsulfonyl)-N-((5-methylpyrazin-2-yl)methyl)-1H-pyrazole-3-carboxamide (example 3; compound 65) The present description discloses the synthesis of exemplary compounds as well as relevant biological activity data (e.g. pages 24 to 47; examples 1 to 3; table 1; compounds 1 to 86).