CAS: 763120-58-7; 1H-Pyrazole-4-Boronic Acid

相似化合物

269410-08-4 1111732-81-0 1188405-87-9

上下游产品

Triisopropyl borate 5-(2-chloro-4-(1H-pyrazol-4-yl)phenyl)-1,3,4-thiadiazol-2-amine

硼酸三异丙酯,4-Iodo-1-(Triisopropylsilyl)-1H-Pyrazole置于正丁基锂体系中,化学反应 0.5H,以72%的收率获得产物4-吡唑硼酸
参考文献:一种氮未取代吡唑和吲唑类硼酸的制备方法
标题:一种氮未取代吡唑和吲唑类硼酸的制备方法
摘要:一种氮未取代吡唑和吲唑类硼酸的制备方法,以氮未取代卤代吡唑及其衍生物或氮未取代卤代吲唑及其衍生物和三异丙基氯硅烷溶于有机溶剂中进行反应,反应生成三异丙基硅基保护的卤代吡唑或者卤代吲唑化合物,再与正丁基锂发生锂溴交换反应,加入硼酸酯引入硼原子,水解后高收率的到得了氮未取代吡唑或吲唑类硼酸.

专利信息

专利号:US-10995078-B2
优先权日:2013-03-13
标 题:Compounds and compositions for inhibition of FASN
发明人：BAIR KENNETH W; LANCIA JR DAVID R; LI HONGBIN; LOCH JAMES; LU WEI; MARTIN MATTHEW W; MILLAN DAVID S; SCHILLER SHAWN E R; TEBBE MARK J
权利人:FORMA THERAPEUTICS INC
摘要:The present invention relates to compounds and composition for inhibition of FASN, their synthesis, applications, and antidotes. An illustrative compound of the invention is shown below:

专利号:WO-2011050245-A1
优先权日:2009-10-23
标 题:Bicyclic heteroaryls as kinase inhibitors
发明人：FENG YANGBO; CHEN YEN TING; SESSIONS HAMPTON; MISHRA JITENDRA K; CHOWDHURY SARWAT; YIN YAN; LOGRASSO PHILIP; LUO JUN-LI; BANNISTER THOMAS; SCHROETER THOMAS
权利人:FENG YANGBO; CHEN YEN TING; SESSIONS HAMPTON; MISHRA JITENDRA K; CHOWDHURY SARWAT; YIN YAN; LOGRASSO PHILIP; LUO JUN-LI; BANNISTER THOMAS; SCHROETER THOMAS
摘要:The invention is directed to heteroaryl compounds useful as inhibitors of various kinase enzymes. In various embodiments, the invention provides a heteroaryl compound having inhibitory bioactivity with respect to a Rho kinase, an AKT kinase, a p70S6K kinase, a LIM kinase, an IKK kinase, a Flt kinase, an Aurora kinase, or a Src kinase, or any combination thereof. Compounds of the invention include bicyclic heteroaryl compounds of formula (I), which can contain a bridging nitrogen atom at a ring junction. The invention further provides methods of synthesis of compounds of the invention, pharmaceutical compositions, pharmaceutical combinations, and methods of treatment of malconditions using compounds of the invention.

专利号:US-9988371-B2
优先权日:2014-06-03
标 题:Benzimidazole analogues and related methods
发明人：LI HONG-YU; FRETT BRENDAN; SANTORO MASSIMO; CARLOMAGNO FRANCESCA
权利人:UNIV ARIZONA; UNIV FEDERICO II; UNIV ARIZONA
摘要:The invention relates to compounds of the formula (VIII) wherein the moieties R 1 , R 2 , R 3 , R 4 , and R 5 are as defined in the specification, and salts thereof, as well as their use, methods of use for them, methods of their synthesis, and the like. The compounds are protein tyrosine kinase inhibitors and can be used in the treatment of various cancer diseases and cancer-associated pain.

专利号:EP-1784396-B8
优先权日:2004-08-26
标 题 :Pyrazole-substituted 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 BICH
权利人:PFIZER
摘要:Compounds of formula (1) are 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.

专利号:WO-2010001220-A1
优先权日:2008-07-01
标 题 :New 1,2,4-triazine derivatives and biological applications thereof
发明人：DESROY NICOLAS; DENIS ALEXIS; GERUSZ VINCENT; OLIVEIRA CHRYSTELLE; VONGSOUTHI VANIDA; MOREAU FRANCOISE; ESCAICH SONIA
权利人:MUTABILIS SA; DESROY NICOLAS; DENIS ALEXIS; GERUSZ VINCENT; OLIVEIRA CHRYSTELLE; VONGSOUTHI VANIDA; MOREAU FRANCOISE; ESCAICH SONIA
摘要:The invention relates to new 1,2,4-triazine derivatives of formula (I): wherein A, B, R2 and Y are defined in the application, their preparation and intermediates, their use as drugs and pharmaceutical compositions and associations containing them. The compounds of formula (I) are capable of inhibiting bacterial heptose synthesis.

专利号:WO-2014024119-A1
优先权日:2012-08-06
标 题:Heterocyclic amides as itk inhibitors
发明人：KUMAR SUKEERTHI; THOMAS ABRAHAM; CHIKHALE RAJENDRA PRAKASH; WAGHMARE NAYAN TATERAO; KADLAG NANASAHEB; KHAIRATKAR-JOSHI NEELIMA; SHAH DAISY MANISH
权利人:GLENMARK PHARMACEUTICALS SA
摘要:The present invention is directed to heterocyclic amide compounds of formula (I) as Tec kinase inhibitors, in particular ITK (interleukin-2 inducible tyrosine kinase) inhibitors. Also provided herein are processes for preparing compounds described herein, intermediates used in their synthesis, pharmaceutical compositions thereof, and methods for treating or preventing diseases, conditions and/or disorders mediated by ITK.