专利号:US-12240835-B2 优先权日:2018-09-18 标题:Substituted benzamides as intermediates in the synthesis of inhibitors of tyrosine kinase enzymatic activity 发明人:ROMERO F ANTHONY; KIRSCHBERG THORSTEN A; HALCOMB RANDALL; XU YINGZI 权利人:TERNS PHARMACEUTICALS INC 摘要:Provided herein are compounds, preferably compounds inhibiting tyrosine kinase enzymatic activity of a protein selected from Abelson protein (ABL1), Abelson-related protein (ABL2), or a chimeric protein BCR-ABL1, compositions thereof, and methods of their preparation, and methods of inhibiting tyrosine kinase enzymatic activity of a protein selected from Abelson protein (ABL1), Abelson-related protein (ABL2), or a chimeric protein BCR-ABL1, and methods for treating diseases wherein modulation of BCR-ABL1 activity prevents, inhibits, or ameliorates the pathology and/or symptomology of the disease. Intermediates such as compounds of Formula (S23), which are useful in the synthesis of compounds inhibiting tyrosine kinase enzymatic activity of a protein selected from Abelson protein (ABL1), Abelson-related protein (ABL2), or a chimeric protein BCR-ABL1, are also provided.
专利号:US-2006047167-A1 优先权日:2004-09-02 标题 :Method of synthesis of water soluble fullerene polyacids using a malonate reactant 发明人:HIRSCH ANDREAS; BEUERLE FLORIAN; CHRONAKIS NIKOS 权利人:HIRSCH ANDREAS; BEUERLE FLORIAN; CHRONAKIS NIKOS 摘要:In one embodiment, the present invention is directed to a method for synthesizing compounds of the formula n n nwhere C m is a fullerene having m carbon atoms, the method comprising the steps of forming a linear malonate compound of the formula n n nwhere each Z is the same or different and is a straight-chain or branched-chain aliphatic radical having from 1-30 carbon atoms which may be unsubstituted or monosubstituted or polysubstituted by identical or different substitutents, in which radicals up to every third —CH 2 — unit can be replaced by O or NR″, n is an integer from 2 to 10, and the unfilled valences of the first and nth malonate groups are filled with bonds to hydrogen, a hydrocarbon group or substituted hydrocarbon group having 1-20 carbon atoms, or a chain containing unsubstituted or substituted aryl or other cyclic groups; or (ii) a branched malonate compound of the formula n n nwhere Z′ is an aliphatic radical having from 1-30 carbon atoms which may be unsubstituted or monosubstituted or polysubstituted by identical or different substitutents, in which radicals up to every third —CH 2 — unit can be replaced by O or NR″; and n is an integer from 2 to 10; n n reacting said malonate compound with C m to form an adduct of the formula n neach Z is bonded to both one carboxylate group of a first malonate moiety and one carboxylate group of a second malonate moiety and the unfilled valences of the first and nth malonate groups are filled with bonds to hydrogen, a hydrocarbon group or substituted hydrocarbon group having 1-20 carbon atoms, or a chain containing unsubstituted or substituted aryl or other cyclic groups; and hydrolyzing said adduct to form the compound.
专利号:WO-2006028776-A1 优先权日:2004-09-02 标题:Method of synthesis of water soluble fullerene polyacids using a malonate reactant 发明人:HIRSCH ANDREAS 权利人:SIXTY INC C; HIRSCH ANDREAS 摘要:A method for synthesizing compounds of the formula (I) where Cm is a fullerene having m carbon atoms and each R is independently -H or -Râ€? COOH where R is alkyl having 1-20 carbon atoms, substituted alkyl having 1-20 carbon atoms, alkenyl having 1-20 carbon atoms, substituted alkenyl having 1-20 carbon atoms, or a chain containing unsubstituted or substituted aryl or other cyclic groups, the method comprising the steps of forming a linear or branched malonate compound and hydrolyzing said adduct to form the compound.
专利号:US-9402842-B2 优先权日:2012-04-13 标题:Synthesis and use of dual tyrosyl-DNA phosphodiesterase I (Tdp1)—topoisomerase I (Top1) inhibitors 发明人:CUSHMAN MARK S; NGUYEN TRUNG X; CONDA-SHERIDAN MARTIN M; POMMIER YVES GEORGE 权利人:PURDUE RESEARCH FOUNDATION 摘要:The invention described herein pertains to the synthesis and use of certain N-substituted indenoisoquinoline compounds which inhibit the activity Tyrosyl-DNA Phosphodiesterase I (Tdp1) or Topoisomerase I (Top1) or both, or otherwise demonstrate anticancer activity. Also disclosed are novel N-substituted indenoisoquinoline compounds and pharmaceutical compositions comprising the novel N-substituted indenoisoquinoline compounds.
专利号:US-2023192718-A1 优先权日:2018-03-30 标 题 :Bicyclic enone carboxylates as modulators of transporters and uses thereof 发明人:SANDANAYAKA VINCENT 权利人:NIROGY THERAPEUTICS INC 摘要:The invention generally relates to the field of monocarboxylate transporter inhibitors, and more particularly to new bicyclic enone carboxylate enone compounds, the synthesis and use of these compounds and their pharmaceutical compositions, e.g., in the treatment, modulation and/or prevention of physiological conditions associated with monocarboxylate transporter activity such as in treating cancer and other neoplastic disorders, tissue and organ transplant rejection.
专利号:US-11027027-B2 优先权日:2015-01-30 标 题:Pyridazinoindole compounds and methods for PET imaging 发明人:MANNING H CHARLES; CHEUNG YIU-YIN; BUCK JASON R; LI JUN 权利人:UNIV VANDERBILT 摘要:Embodiments of the invention include a novel synthesis of the translocator protein (TSPO) ligands, and methods of imaging a molecular events. Also disclosed are compounds for treatment of diseases, including cancer.
摘要:von Angerer, S., Science of Synthesis Knowledge Updates, (2011) 1, 224. 参考文献:10.1007/bf02975090 摘要:Hwang KJ, Lee TS, Kim KW, Kim BT, Lee CM, Park EY, Woo RS. 4-Hydroxy-6-oxo-6,7-dihydro-thieno[2,3-b] pyrimidine derivatives: synthesis and their biological evaluation for the glycine site acting on the N-methyl-D-aspartate (NMDA) receptor. Arch Pharm Res. 2001 Aug;24(4):270–5. doi: 10.1007/bf02975090.