专利号:US-2023405565-A1 优先权日:2022-06-21 标 题:Catalyst composition for biaryl synthesis by decarboxylative cross-coupling 发明人:LIM CHERN-HOOI; QIAN GANG; ELDER WILLIAM ZACHARY; RILEY PAIGE; KOLVENBACH ROBIN; WALTER PHILIPP; GOCK MICHAEL 权利人:HERAEUS DEUTSCHLAND GMBH & CO KG; NEW IRIDIUM INC 摘要:The present invention relates to a catalyst composition for synthesis of heteroaromatic biaryls by a light-assisted decarboxylative carbon-carbon cross-coupling reaction, wherein the composition comprises(i) a palladium compound which is selected from a palladium salt or a palladium complex or a mixture thereof,(ii) at least one of the following compounds:a compound of Formula (I)a compound of Formula (II)an iridium complex comprising ligands L1, L2 and L3, wherein the ligands L1, L2 and L3 are selected, independently from each other, from a phenylpyridine and a bipyridine.
专利号:US-2003157061-A1 优先权日:2001-12-05 标 题 :Combinations of a cyclooxygenase-2 selective inhibitor and a TNFalpha antagonist and therapeutic uses therefor 发明人:BENNETT DENNIS A 权利人:PHARMACIA CORP 摘要:A method for the prevention, treatment, or inhibition of pain, inflammation, or inflammation-related disorder and for the prevention, treatment, or inhibition of a cardiovascular disease or disorder in a subject that is in need of such prevention, treatment or inhibition, involves the administration to the subject of a cyclooxygenase-2 selective inhibitor or prodrug thereof and a TNFα antagonist. A method can also involve the treatment, prevention, or inhibition of cancer in a subject in need of such treatment, prevention, or inhibition, by administering to the subject a cyclooxygenase-2 selective inhibitor or prodrug thereof and a TNFα antagonist which is selected from the group consisting of a compound that affects the synthesis of TNFα, a compound that inhibits the binding of TNFα with a receptor specific for TNFα, and a compound that interferes with intracellular signaling triggered by TNFα binding with a receptor. Compositions, pharmaceutical compositions and kits that can be used with the methods are also described.
专利号:WO-2004087679-A1 优先权日:2003-04-01 标 题 :2, 4, 6-trisubstituted pyrimidine derivatives useful for the treatment of neoplastic and autoimmune diseases 发明人:OBRECHT DANIEL; ERMERT PHILIPP; LUTHER ANATOL; EBERLE MARTIN; BACHMANN FELIX 权利人:APONETICS AG; OBRECHT DANIEL; ERMERT PHILIPP; LUTHER ANATOL; EBERLE MARTIN; BACHMANN FELIX 摘要:The invention relates to substituted pyrimidines of formula (I) wherein V represents a bond or CR6R7, W represents a bond, NR8 or oxygen, X represents sulfur, or nitrogen substituted by hydrogen or R5, Y represents -CH2-, -CH2CH2-, -CO- or -CS-, R1 represents unsubstituted or substituted aryl or heteroaryl, and the substituents R2, R3, R4, R5, R6, R7 and R8 have the meanings given in the specification. These compounds are selectively inducing apoptosis in cancer cells and can be used for the treatment of neoplastic and autoimmune diseases. The invention relates also to methods of synthesis of such compounds, to their use as medicaments, to pharmaceutical compositions containing same, and to methods of treatment of neoplastic and autoimmune diseases using such compounds of formula (I) or of pharmaceutical compositions containing same.
专利号:US-2004110228-A1 优先权日:2002-04-01 标 题:Combinatorial organic synthesis of unique biologically active compounds 发明人:MCALPINE SHELLI R; TAYLOR RACHEL E; BOLLA MEGAN L; SEGALL ANCA M 摘要:The invention provides a method for making a combinatorial library of cyclic compounds, such as Holliday junction-trapping compounds, comprising the steps of (a) obtaining a plurality of trimers according to the generic structure X 1- X 2- X 3 , wherein X 1 , X 2 and X 3 can be independently any naturally or nonnaturally occurring amino acids or peptidomimetics thereof; (b) optionally coupling a spacer S to the trimer at either end; (c) cyclizing two trimers or trimer-spacer conjugates in a head-to-tail orientation; thereby obtaining a combinatorial library of compounds, wherein the library does not include an unmodifed or naturally occurring Holliday Junction-trapping compounds. The invention additionally provides methods macrocyclic compounds that are synergimycin derivatives.
专利号:US-7161024-B2 优先权日:2003-07-10 标题 :Process for the preparation and purification of 2-(alkoxyalkylidene)-3-ketoalkanoic acid esters from 3-ketoalkanoic acid esters 发明人:DRAPER RICHARD W 权利人:SCHERING CORP 摘要:In its several embodiments, this invention discloses a novel process to prepare the compounds of Formula 3: n nwherein R 1 is lower alkyl, and R 2 and R 3 can be the same or different, each being independently selected from the group consisting of alkyl, aryl and aralkyl; said process being carried out in a suitable solvent with at least one tert-amine carboxylate salt catalyst. The compounds of formula 3 are chemical intermediates useful for the synthesis of various heterocyclic compounds. These heterocyclic compounds are in turn useful precursors for diverse pharmaceutical, herbicidal and insecticidal agents. In particular, these intermediates are useful precursors to a variety of CCR5 inhibitors.
专利号:US-9676783-B2 优先权日:2008-10-22 标 题:Method of treatment using substituted pyrazolo[1,5-A] pyrimidine compounds 发明人:HAAS JULIA; ANDREWS STEVEN W; JIANG YUTONG; ZHANG GAN 权利人:ARRAY BIOPHARMA INC 摘要:Compounds useful in the synthesis of compounds for treating pain, cancer, inflammation, neurodegenerative disease or Typanosoma cruzi infection in a mammal.
摘要:S. F. Mason. J. Chem. Soc. 1959, 1247. 参考文献:10.1107/s1600536810027030 摘要:Zhao J, Liu F. Poly[tetra-μ1,1-azido-bis(μ2-pyrimidine-2-carboxylato)tricopper(II)]. Acta Crystallogr E Struct Rep Online. 2010 Jul 21;66(8):m973. doi: 10.1107/s1600536810027030. 参考文献:10.1107/s1600536810030023 摘要:Zhao JP, Liu FC. catena-Poly[[(pyrimidine-2-carb-oxy-lic acid)iron(II)]-μ-oxalato]. Acta Crystallogr Sect E Struct Rep Online. 2010 Aug 04;66(Pt 9):m1059. 参考文献:10.1007/s11064-014-1336-9 摘要:Al-Khawaja A, Petersen JG, Damgaard M, Jensen MH, Vogensen SB, Lie ME, Kragholm B, Bräuner-Osborne H, Clausen RP, Frølund B, Wellendorph P. Pharmacological identification of a guanidine-containing β-alanine analogue with low micromolar potency and selectivity for the betaine/GABA transporter 1 (BGT1). Neurochem Res. 2014 Oct;39(10):1988–96. doi: 10.1007/s11064-014-1336-9. 参考文献:10.1104/pp.108.120519 摘要:Shimizu M, Goto M, Hanai M, Shimizu T, Izawa N, Kanamoto H, Tomizawa K, Yokota A, Kobayashi H. Selectable tolerance to herbicides by mutated acetolactate synthase genes integrated into the chloroplast genome of tobacco. Plant Physiol. 2008 Aug;147(4):1976–83.