专利号:US-2003083352-A1 优先权日:2000-07-31 标 题 :Synthesis of imidazole intermediates 发明人:HELAL CHRISTOPHER J 权利人:PFIZER 摘要:The invention provides a method for synthesis of compounds of formula n n n wherein R 1 and R 19 are as defined. Compounds of formula 12 are useful as intermediates for synthesizing compounds having pharmacological activity inhibiting cdk5, cdk2, and GSK-3.
专利号:WO-2018175954-A1 优先权日:2017-03-23 标 题 :Synthesis of imidazo[5,1-a]isoindole derivative useful as ido inhibitors 发明人:ANGELAUD REMY; BACHMANN STEPHAN; BEYELER ANDREAS; CARRERA DIANE; FISCHER ROLF; GUILLEMONT-PLASS MAUD; HOU HAIYUN; IDING HANS; KRAFT ANNE KATRIN; MANNS ANDREAS; MEIER ROLAND; NIEDERMANN KARIN; OLBRICH MARTIN; PIECHOWICZ KATARZYNA; REGE PANKAJ; REMARCHUK TRAVIS; SIROIS LAUREN; ST-JEAN FREDERIC; XU JIE 权利人:HOFFMANN LA ROCHE; HOFFMANN LA ROCHE; GENENTECH INC 摘要:Presently provided is a method of making a compound of the Formula (I) wherein X is halogen, which is useful for modulating the activity of indoleamine 2,3-dioxygenase (IDO) and treating diseases and conditions in which the inhibition of IDO mediated immunosuppression is beneficial.
专利号:US-10947203-B2 优先权日:2016-03-25 标题 :1,4,5-substituted 1,2,3-triazole analogues as antagonists of the pregnane X receptor 发明人:CHEN TAOSHENG; LIN WENWEI; WANG YUEMING 权利人:ST JUDE CHILDRENS RES HOSPITAL; ST JUDE CHILDRENS RSEARCH HOSPITAL 摘要:In an aspect, the invention relates to 1,4,5-substituted 1,2,3-triazole and 1,2,4,5-substituted imidazoles having a structure represented by a formula: n nwhich are modulators the pregnane X receptor (“PXRâ€?); synthesis methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of modulating an adverse drug reaction in a mammal using the compounds and pharmaceutical compositions; methods of treatment of a disorder of uncontrolled cellular proliferation, such as a cancer, using the compounds and pharmaceutical compositions; methods of modulating pregnane X receptor activity in a mammal using the compounds and pharmaceutical compositions. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.
专利号:WO-2024041555-A1 优先权日:2022-08-24 标 题:Methods of manufacturing kinase inhibitors 发明人:LIANG XING; CAO HUA; CHENG XIN; QIN LUOHENG 权利人:INSILICO MEDICINE IP LTD 摘要:In one aspect, the disclosure provides methods of synthesizing TNIK and/or MAP4K4 kinases inhibitors for the treatment of disease. In one aspect, the disclosure provides intermediates used in the synthesis methods described herein.
专利号:HU-T78019-A 优先权日:1995-03-31 标 题 :A method for the synthesis of substituted nitrogen-containing heterocyclic compounds
专利号:US-8785632-B2 优先权日:2004-08-26 标 题:Enantiomerically pure aminoheteroaryl compounds as protein kinase inhibitors 发明人:CUI JINGRONG JEAN; FUNK LEE ANDREW; JIA LEI; KUNG PEI-PEI; MENG JERRY JIALUN; NAMBU MITCHELL DAVID; PAIRISH MASON ALAN; SHEN HONG; TRAN-DUBE MICHELLE 权利人:CUI JINGRONG JEAN; FUNK LEE ANDREW; JIA LEI; KUNG PEI-PEI; MENG JERRY JIALUN; NAMBU MITCHELL DAVID; PAIRISH MASON ALAN; SHEN HONG; TRAN-DUBE MICHELLE; AGOURON PHARMA; PFIZER 摘要:Enantiomerically pure compound of formula 1 n nare provided, as well as methods for their synthesis and use. Preferred compounds are potent inhibitors of the c-Met protein kinase, and are useful in the treatment of abnormal cell growth disorders, such as cancers.
摘要:Nelson, D. J., Science of Synthesis: N-Heterocyclic Carbenes in Catalytic Organic Synthesis, (2016) 2, 283. 摘要:G.B. Barlin. J. Chem. Soc., B 1967, 641. 摘要:Kleemann A., Kutscher B., Reichert D., Bossart M., Pharmaceutical Substances, Thieme [Online], Stuttgart, (2026). 参考文献:10.1021/bi049077g 摘要:Cao W, Ye X, Sjodin T, Christian JF, Demidov AA, Berezhna S, Wang W, Barrick D, Sage JT, Champion PM. Investigations of photolysis and rebinding kinetics in myoglobin using proximal ligand replacements. Biochemistry. 2004 Aug 31;43(34):11109–17. doi: 10.1021/bi049077g.