专利号:US-5693792-A 优先权日:1992-02-18 标 题 :β-lactam and cephem compounds and processes for their production 发明人:TORII SHIGERU; TANAKA HIDEO; SASAOKA MITIO; SHIROI TAKASHI; KAMEYAMA YUTAKA 权利人:OTSUKA KAGAKU KK 摘要:The object of the invention is to provide a β-lactam compound and a 2-substituted methyl-3-cephem compound, both of which are of value as intermediates for the synthesis of cephem antibiotics. n The β-lactam compound of the invention may be represented by the general formula ##STR1## wherein R 1 represents a protected amino group, for instance; R 2 represents hydrogen, for instance; R 3 represents hydrogen or a carboxy-protecting group; R 4 represents an aryl group which may be substituted; R 5 represents an alkenyl group which may be substituted, for instance. The 2-substituted methyl-3-cephem compound of the invention may be represented by the general formula ##STR2## wherein R 1 , R 2 and R 3 are as defined above; R 6 represents an aryl group which may be substituted.
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-2024343719-A1 优先权日:2017-03-17 标题 :Kappa opioid receptor antagonists and products and methods related thereto 发明人:ROBERTS EDWARD; GUERRERO MIGUEL A; URBANO MARIANGELA; ROSEN HUGH; JONES ROBERT M; LAXAMANA CANDACE MAE; ZHAO XIANRUI; TURTLE ERIC DOUGLAS 权利人:SCRIPPS RESEARCH INST; BLACKTHORN THERAPEUTICS INC 摘要:Compounds are provided that antagonize the kappa-opioid receptor (KOR) and products containing such compounds, as well as to methods of their use and synthesis. Such compounds have the structure of Formula (I), or a pharmaceutically acceptable isomer, racemate, hydrate, solvate, isotope or salt thereof: n n n n n n n n n n wherein X, Y, R 1 , R 2 , R 4 , R 5 R 6 , R 7 , R 8 and R 11 are as defined herein.
专利号:US-11897873-B2 优先权日:2017-03-17 标 题:Kappa opioid receptor antagonists and products and methods related thereto 发明人:ROBERTS EDWARD; GUERRERO MIGUEL A; URBANO MARIANGELA; ROSEN HUGH; JONES ROBERT M; LAXAMANA CANDACE MAE; ZHAO XIANRUI; TURTLE ERIC DOUGLAS 权利人:SCRIPPS RESEARCH INST; BLACKTHORN THERAPEUTICS INC 摘要:Compounds are provided that antagonize the kappa-opioid receptor (KOR) and products containing such compounds, as well as to methods of their use and synthesis. Such compounds have the structure of Formula (I), or a pharmaceutically acceptable isomer, racemate, hydrate, solvate, isotope or salt thereof:wherein X, Y, R1, R2, R4, R5, R6, R7, R8 and R11 are as defined herein.
专利号:US-12404250-B2 优先权日:2018-08-27 标 题:PARP inhibitors for treating cancer and asthma 发明人:COHEN MICHAEL; KIRBY ILSA 权利人:UNIV OREGON HEALTH & SCIENCE 摘要:Provided are substituted 8-methylquinazolin-4(3H)-one compounds useful as PARP inhibitors for the treatment of cancer and asthma, as well as pharmaceutical compositions comprising them and methods for their synthesis.
摘要:Celik, I.; Hummel, S.; Kirsch, S. F., Science of Synthesis Knowledge Updates, (2019) 1, 34. 摘要:Patil, N. T.; Tathe, A. G.; Bhoyare, V. W., Science of Synthesis, (2019) , 127.