专利号:US-11512097-B2 优先权日:2019-11-25 标题 :Heterocyclic compounds as Delta-5 desaturase inhibitors and methods of use 发明人:ALLEN JENNIFER R; BELTRANI MICHELA; BOURBEAU MATTHEW P; DAMYANOVA TEODORA P; LINGARD IAIN; MINATTI ANA E; VINCETTI PAOLO 权利人:AMGEN INC 摘要:The present disclosure provides compounds useful for the inhibition of Delta-5 Desaturase (“D5Dâ€?). The compounds have a general Formula I n nwherein the variables of Formula I are defined herein. This disclosure also provides pharmaceutical compositions comprising the compounds, uses of the compounds, and compositions for treatment of, for example, a metabolic or cardiovascular disorder. Further, the disclosure provides intermediates useful in the synthesis of compounds of Formula I.
专利号:US-4395561-A 优先权日:1982-05-14 标 题 :Synthesis of 3-hydroxyoxetane 发明人:BAUM KURT; GRAKAUSKAS VYTAUTAS; BERKOWITZ PHILLIP T 权利人:US NAVY 摘要:A process for preparing 3-hydroxyoxetane comprising the following steps in order n (1) reacting a carboxylic acid of the formula CH 3 (CH 2 ) n COOH with epichlorohydrin in the presence of anhydrous ferric chloride to produce an ester of the formula ##STR1## wherein n is an integer of from 0 to 3; (2) protecting the secondary hydroxy group of the ester with a blocking group, Z, that is stable to bases; thus forming a blocked ester of the formula ##STR2## (3) hydrolyzing the blocked ester formed in step (2) with an aqueous base to remove the carboxylic acid and form a 3-hydroxyoxetane derivative of the formula ##STR3## in which Z represents the blocking group; (4) removing the blocking group from the 3-hydroxyoxetane derivative by heating it with an alcohol and an acid to form the product 3-hydroxyoxetane, ##STR4##
专利号:US-8030440-B1 优先权日:2010-05-21 标 题 :Synthesis of poly-(3-nitratooxetane) 发明人:WILLER RODNEY L; BAUM KURT; LIN WEN-HUEY 权利人:FLUOROCHEM INC 摘要:3-nitratooxetane. n Poly-(3-nitratooxetane). n The method of synthesizing 3-nitratooxetane comprising reacting 3-hydroxyoxetane with a nitration agent. n The method of synthesizing poly-(3-nitratooxetane) by polymerizing 3-nitratooxetane using a polyol initiator.
专利号:US-12150934-B2 优先权日:2016-11-30 标 题 :Methods of using substituted pyrazole and pyrazole compounds and for treatment of hyperproliferative diseases 发明人:SIDDIQUI ARSHAD M; CIBLAT STEPHANE; CONSTANTINEAU-FORGET LEA; GRAND-MAITRE CHANTAL; GUO XIANGYU; SRIVASTAVA SANJAY; SHIPPS GERALD W; COOPER ALAN B; OZA VIBHA; KOSTURA MATTHEW W; LUTHER MICHAEL; LEVINE JEDD 权利人:BANTAM PHARMACEUTICAL LLC 摘要:Disclosed are methods of treating hyperproliferative disorders such as cancer, methods of arresting the cell cycle in cancer cells, methods of inhibiting glutathione synthesis in cancer cells, and associated compounds for use and uses in medicaments. In certain embodiments, the methods, uses and compounds are provided with reference to compounds of the structural formula (I), in which X1, X2, Z1, Z2, the ring system denoted by “aâ€?, R1, L1, L2, Q, L3, R3, L4, R4, L5, and R5 are as described herein. In certain embodiments, compounds disclosed herein are especially active against cancers having a mutant KRAS gene.
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-2024409557-A1 优先权日:2023-05-09 标 题 :5,6-fused and 6,6-fused bicyclic alcohols and ethers and compositions for use as 15-prostaglandin dehydrogenase modulators 发明人:GREENMAN KEVIN LLOYD; PICKRELL ALEXANDER J; LI KEXUE; AMEGADZIE ALBERT K; WANG HUI-LING; WEIRES NICHOLAS ANTHONY; ALLEN JOHN G; BOURBEAU MATTHEW P 权利人:AMGEN INC 摘要:The present disclosure provides novel 15-hydroxy-prostaglandin dehydrogenase inhibitors, pharmaceutical compositions comprising such compounds, and methods of using such compounds and compositions in treating 15-hydroxy-prostaglandin dehydrogenase-mediated disease. Also provided are methods of making such compounds and intermediates thereof. The compounds have a general Formula (A).Further, the disclosure provides intermediates useful in the synthesis of compounds of Formula (A).
摘要:Croft, R. A.; Bull, J. A., Science of Synthesis Knowledge Updates, (2018) 4, 424. 摘要:Shu, X.-Z.; Pang, X., Science of Synthesis: Special Topics, (2022) 1, 430.