专利号:EP-3325432-B1 优先权日:2015-07-24 标题:Methods of synthesis of (1r,2r,5r)-5-amino-2-methylcyclohexanol hydrochloride and intermediates useful therein
专利号:WO-2017019487-A1 优先权日:2015-07-24 标 题:Methods of synthesis of (1r,2r,5r)-5-amino-2-methylcyclohexanol hydrochloride and intermediates useful therein
专利号:WO-2023091726-A1 优先权日:2021-11-18 标题:Inhibitors of cyclin‑dependent kinase 12 (cdk12) 发明人:BENOIT GUILLAUME; CARULLI JOHN; CHEN FEI; CHUAQUI CLAUDIO; CIBLAT STEPHANE; COOPER ELLIOT; DAGENAIS ROBIN; HU SHANHU; KABRO ANZHELIKA; LAPLACA DEREK; MARINEAU JASON; MOEBIUS DAVID; MOON DIANE; SOLODININ ANDREI; WHITMORE KENNETH 权利人:SYROS PHARMACEUTICALS INC 摘要:The present invention provides chemical compounds that inhibit one or more families of kinases (e.g., serine/threonine kinases, including one or more of the families of CDK proteins, and in particular, CDK12). More specifically, the present invention provides CDK12 inhibitors, of formula (I), pharmaceutically acceptable salts and isotopically labeled derivatives thereof, pharmaceutical compositions containing the compounds/inhibitors, and methods of their synthesis and use in treating proliferative diseases (e.g., a bladder cancer, a breast cancer, Ewing's sarcoma, a gastric cancer, a gastrointestinal cancer, a hematologic cancer, a lung cancer (e.g., small cell lung cancer (SCLC)), an ovarian cancer (e.g., a high grade serous ovarian cancer), a pancreatic cancer (e.g., pancreatic ductal adenocarcinoma (PDAC)), a brain cancer (e.g., glioblastoma), or a prostate cancer), alone or in combination with a second therapeutic agent. The proliferative disease can be a cancer, benign neoplasm, or pathologic angiogenesis, and any of the therapeutic methods or uses described herein can include a step of diagnosing the patient's disease. In other embodiments of the invention, the compositions described herein (e.g., the compounds, pharmaceutical compositions, and kits containing them) are used for the treatment of myotonic dystrophy (type 1 or type 2).
专利号:US-9370515-B2 优先权日:2013-03-07 标题 :Mixed lineage kinase inhibitors and method of treatments 发明人:GOODFELLOW VAL S; NGUYEN THONG X; RAVULA SATHEESH B; GELBARD HARRIS A 权利人:CALIFIA BIO INC; UNIV ROCHESTER 摘要:Provided herein are imidazopyridine compounds having an inhibitory effect on mixed lineage kinases (MLKs), methods of their synthesis, and methods of their therapeutic. Also provided are pharmaceutical compositions comprising the compounds and methods of using the compounds and pharmaceutical compositions.
专利号:EP-3795553-A1 优先权日:2015-07-24 标 题 :Methods of synthesis of (1r,2r,5r)-5-amino-2-methylcyclohexanol hydrochloride and intermediates useful therein
专利号:CN-116102543-A 优先权日:2022-10-21 标题 :A kind of GLP-1R agonist, synthesis method and use thereof
参考文献:10.1016/j.saa.2011.02.010 摘要:de Oliveira PR, Viesser RV, Guerrero PG, Rittner R. Influence of OH⋯N and NH⋯O inter- and intramolecular hydrogen bonds in the conformational equilibrium of some 1,3-disubstituted cyclohexanes through NMR spectroscopy and theoretical calculations. Spectrochimica Acta Part A: Molecular and Biomolecular Spectroscopy. 2011 May;78(5):1599–605. doi: 10.1016/j.saa.2011.02.010.