4-Iodo-1-Methyl-3-Nitropyrazole置于盐酸,Tin(Ll) Chloride体系中,用 水 用作溶剂,化学反应 2.0H,以51%的收率获得n-甲基-3-氨基吡唑 参考文献:Synthesis Of Vicinal Aminoiodo-And (Acetylamino)Iodo-L-Alkylpyrazoles 标题:Synthesis Of Vicinal Aminoiodo-And (Acetylamino)Iodo-L-Alkylpyrazoles 摘要:3-And 5-(Acetylamino)-4-Iodo-1-Alkylpyrazoles Were Obtained By Successive Acylation And Iodination From 3-And 5-Amino-1-Alkylpyrazoles Without Isolating Intermediate (Acetylamino)Pyrazoles. 3-And 5-Iodo-And 3,5-Diiodo-4-Amino-1-Methylpyrazoles Were Synthesized From Appropriate Iodonitropyrazoles By Reduction With Sncl2 In Hcl. Doi:10.1007/bf01431121
专利信息
专利号:US-11512097-B2 优先权日:2019-11-25 标题 :Heterocyclic compounds as Delta-5 desaturase inhibitors and methods of use 发明人:ALLEN JENNIFER R; BELTRANI MICHELA; BOURBEAU MATTHEW P; DAMYANOVA TEODORA P; LINGARD IAIN; MINATTI ANA E; VINCETTI PAOLO 权利人:AMGEN INC 摘要:The present disclosure provides compounds useful for the inhibition of Delta-5 Desaturase (“D5Dâ€?). The compounds have a general Formula I n nwherein the variables of Formula I are defined herein. This disclosure also provides pharmaceutical compositions comprising the compounds, uses of the compounds, and compositions for treatment of, for example, a metabolic or cardiovascular disorder. Further, the disclosure provides intermediates useful in the synthesis of compounds of Formula I.
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-11731956-B2 优先权日:2018-10-22 标 题:Substituted 1,2,4-triazoles as intermediates in the synthesis of TYK2 inhibitors
专利号:US-7427625-B2 优先权日:2006-02-08 标 题 :Substituted thiatriazaacenaphthylene-6-carbonitrile kinase inhibitors 发明人:CONNOLLY PETER J; EMANUEL STUART L; HAYDEN STUART; JOHNSON SIGMOND G; LAGU BHARAT; MIDDLETON STEVEN A; PANDEY NIRANJAN B; POWELL MARK T 权利人:JANSSEN PHARMACEUTICA NV 摘要:The present invention is directed to substituted thiatriazaacenaphthylene-6-carbonitrile compounds of formula (I): n nand forms thereof, their synthesis and use for treating, preventing or ameliorating a chronic or acute protein kinase mediated disease, disorder or condition.
摘要:Hay, M. B.; Hicks, J. D., Science of Synthesis: Cross Coupling and Heck-Type Reactions, (2012) 2, 161. 摘要:Graham, J. S.; Stanway-Gordon, H. A.; Waring, M. J., Science of Synthesis: DNA-Encoded Libraries, (2024) nan, 431. 摘要:Graham, J. S.; Stanway-Gordon, H. A.; Waring, M. J., Science of Synthesis: DNA-Encoded Libraries, (2024) nan, 438.