CAS: 31462-59-6; Pyrimidine-4-Carboxylic Acid

上下游产品

CAS号3438-46-8 4-甲基嘧啶 | CAS号49689-16-9 [1,2,3]-triazol... | CAS号50593-92-5 5-溴-2-(甲巯基)-4-嘧啶甲酸 | CAS号5424-21-5 2,4-二氯-6-甲基嘧啶 | CAS号626-48-2 6-甲基尿嘧啶 | CAS号184951-32-4 4-嘧啶羰酰氯 | CAS号28648-86-4 嘧啶-4-甲酰胺 | CAS号289-95-2 嘧啶 | CAS号2450-08-0 嘧啶-4-甲酸甲酯 | CAS号62846-82-6 4-嘧啶甲酸乙脂 | CAS号503860-53-5 2,3-二氢-1-甲基-2-硫... | CAS号503860-54-6 2-氯-1-甲基-[4,4-B...

4-甲基嘧啶置于吡啶,Selenium(Iv) Oxide体系中,化学反应 6.0H,以19%的收率获得产物4-嘧啶甲酸
参考文献:高选择性和有效的g蛋白偶联受体激酶2(grk2)抑制剂的设计,合成和评估,可用于治疗心力衰竭
标题:高选择性和有效的g蛋白偶联受体激酶2(grk2)抑制剂的设计,合成和评估,可用于治疗心力衰竭
摘要:用于心力衰竭的一类新型治疗药物,高效和选择性的grk2抑制剂,在体外研究中表现出增强的β-肾上腺素信号传导能力.hts将衍生物5和1,2,4-三唑衍生物24A鉴定为命中化合物.新一代的脚手架和所有部分的sar研究都产生了带有n-苄基羧酰胺部分的4-甲基-1,2,4-三唑衍生物,对grk2的活性很高,对其他激酶的选择性更高.在亚型选择性方面,这些化合物对grk1,5,6和7表现出足够的选择性,并且对grk3具有几乎相同的抑制作用.我们的药物化学努力导致发现了115H(grk2 Ic 50= 18 Nm),获得了与人grk2和grk2抑制剂的共晶体结构,该抑制剂增强了β-肾上腺素能受体(βar)介导的camp积累,并防止了用异丙肾上腺素处理过的表达β2Ar的hek293细胞中βar的内在化.因此,115H似乎是心力衰竭治疗的一种新型疗法.
DOI:10.1021/acs.Jmedchem.7B00443

专利信息

专利号:US-12006324-B1
优先权日:2022-12-15
标题:Preparation method of trilaciclib and precursors of trilaciclib
发明人：KAMANI SATYANARAYANA; CHANG HSIN-YUN; LU TZU-CHIANG; MAI CHIN-CHENG
权利人:CHUNGHWA CHEMICAL SYNTHESIS & BIOTECH CO LTD
摘要:Disclosed herein is a specific method of preparation of Trilaciclib. The said method is to provide an efficacy of a protection free synthetic method of Trilaciclib with less steps and good yields.

专利号:WO-2025128848-A1
优先权日:2023-12-12
标题:Heterocyclic compounds as triggering receptor expressed on myeloid cells 2 agonists and methods of use
发明人：HOUZE JONATHAN B; PANDYA BHAUMIK
权利人:VIGIL NEUROSCIENCE INC
摘要:The present disclosure provides compounds of Formula (I), useful for the activation of Triggering Receptor Expressed on Myeloid Cells 2 ('TREM2'). This disclosure also provides pharmaceutical compositions comprising the compounds, uses of the compounds, and compositions for treatment of, for example, a neurodegenerative disorder. Further, the disclosure provides intermediates useful in the synthesis of compounds of Formula (I).

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-2010004245-A1
优先权日:2006-10-20
标 题:Azacycloalkane derivatives as inhibitors of stearoyl-coenzyme a delta-9 desaturase
发明人：OBALLA RENATA M; DESCHENES DENIS; GAGNON MARC; LEBLANC YVES; POWELL DAVID; RAMTOHUL YEEMAN K
权利人:MERCK FROSST CANADA LTD
摘要:Azacycloalkane derivatives of structural formula (I) are selective inhibitors of stearoyl-coenzyme A delta-9 desaturase (SCD1) relative to other known stearoyl-coenzyme A desaturases. The compounds of the present invention are useful for the prevention and treatment of conditions related to abnormal lipid synthesis and metabolism, including cardiovascular disease, such as atherosclerosis; obesity; diabetes; neurological disease; metabolic syndrome; insulin resistance; and liver steatosis.

专利号:US-5169935-A
优先权日:1990-06-20
标 题:Method of making peptides
发明人：HOEGER CARL A; THEOBALD PAULA G; PORTER JOHN S; RIVIER JEAN E F
权利人:SALK INST FOR BIOLOGICAL STUDI
摘要:Methods for making peptides of a suitable length for solid phase synthesis, which peptides include in their sequence a pair of residues of a different character which have acylated side chains and a residue which has an N-alkylated side chain. A peptide intermediate is constructed on the resin using commercially available starting materials. The N-terminus can be acylated by removing the alpha -amino protecting group and acylating under standard conditions. First primary amino protecting groups included in those residues to be acylated are removed, and acylation is effected, preferably by using a carboxypyridine or a similar heterocyclic acylating agent. Following such side chain acylation, a second protecting group included in the residue to be N-alkylated is removed, and the N-alkylation reaction is carried out while the peptide remains on the resin using a borohydride and an appropriate aldehyde or ketone. Following cleavage from the resin and removal of any protecting groups still remaining, the peptide is appropriately purified, thus requiring only a single purification to be carried out while forming a synthetic peptide including residues for which the modified amino acids are not readily commercially available.