专利号:US-9221821-B2 优先权日:2012-06-05 标题:Methods for the synthesis of 1,3-substituted aminouracils and other xanthine-related compounds 发明人:DIEP NHUT; KALYAN YURIY B 权利人:FOREST LAB HOLDINGS LTD; FOREST LAB HOLDINGS LTD 摘要:Methods for the synthesis of disubstituted aminouracils and xanthine and/or xanthine-related compounds are provided.
专利号:WO-2023086801-A1 优先权日:2021-11-09 标题 :Heterocyclic compounds as triggering receptor expressed on myeloid cells 2 agonists and methods of use 发明人:HOUZE JONATHAN B; PANDYA BHAUMIK; KAPLAN ALAN P; BOS MAXENCE; MANCUSO JOHN; FRANZONI IVAN 权利人:VIGIL NEUROSCIENCE INC 摘要:The present disclosure provides compounds of Formula I, useful for the activation of Triggering Receptor Expressed on Myeloid Cells 2 ('TREM2'). This disclosure also provides pharmaceutical compositions comprising the compounds, uses of the compounds, and compositions for treatment of, for example, a neurodegenerative disorder. Further, the disclosure provides intermediates useful in the synthesis of compounds of Formula I.
专利号:US-9676783-B2 优先权日:2008-10-22 标 题:Method of treatment using substituted pyrazolo[1,5-A] pyrimidine compounds 发明人:HAAS JULIA; ANDREWS STEVEN W; JIANG YUTONG; ZHANG GAN 权利人:ARRAY BIOPHARMA INC 摘要:Compounds useful in the synthesis of compounds for treating pain, cancer, inflammation, neurodegenerative disease or Typanosoma cruzi infection in a mammal.
专利号:EP-3904354-A1 优先权日:2020-04-30 标 题:New imidazolone derivatives as inhibitors of protein kinases in particular dyrk1a, clk1 and/or clk4 权利人:PERHA PHARMACEUTICALS 摘要:The present invention relates to a compound of formula (I)n nwherein R 1 represents a (C 1 -C 6 )alkyl group, a spiro(C 5 -C 11 )bicyclic ring, a fused phenyl group, a substituted phenyl group, a R'-L- group, wherein L is either a single bond or a (Ci-C3)alkanediyl group, and R' represents a (C 3 -C 8 )cycloalkyl group, a bridged (C6-C 10 )cycloalkyl group, a (C 3 -C 8 )heterocycloalkyl group, or a (C 3 -C 8 )heteroaryl group, or a R'-L- group wherein L is a (Ci-C3)alkanediyl group, and R' is a an optionally substituted phenyl group or any of its pharmaceutically acceptable salt. n The present invention further relates to a composition comprising a compound of formula (I) and a process for manufacturing said compound as well as its synthesis intermediates. n It also relates to said compound for use as a medicament, in particular in the treatment and/or prevention of cognitive deficits associated with Down syndrome; Alzheimer's disease; dementia; tauopathies; Parkinson's disease; CDKL5 Deficiency Disorder; Phelan-McDermid syndrome; autism; diabetes; regulation of folate and methionine metabolism; osteoarthritis; Duchenne muscular dystrophy; several cancers; neuroinflammation, anemia and infections and for regulating body temperature.
专利号:US-8987195-B2 优先权日:2012-08-08 标 题:HCV NS3 protease inhibitors 发明人:BARA THOMAS; BHAT SATHESH; BISWAS DIPSHIKHA; BROCKUNIER LINDA; BURNETT DUANE A; CHACKALAMANNIL SAMUEL; CHELLIAH MARIAPPAN V; CHEN AUSTIN; CLASBY MARTIN; COLANDREA VINCE J; GUO ZHUYAN; HAN YONGXIN; JAYNE CHARLES; JOSIEN HUBERT; MARCANTONIO KAREN; MIAO SHOUWU; NEELAMKAVIL SANTHOSH; PINTO PATRICK; RAJAGOPALAN MURALI; SHAH UNMESH; VELAZQUEZ FRANCISCO; VENKATRAMAN SRIKANTH; XIA YAN 权利人:MERCK SHARP & DOHME; MERCK CANADA INC 摘要:The present invention relates to hepatitis C virus (HCV) NS3 protease inhibitors containing a spirocyclic moeity, uses of such compounds, and synthesis of such compounds.
专利号:US-8466287-B2 优先权日:2005-06-09 标题 :Process for producing tricyclic ketone 发明人:NISHIYAMA HIROYUKI; SAWADA SEIGO 权利人:NISHIYAMA HIROYUKI; SAWADA SEIGO; YAKULT HONSHA KK 摘要:In order to efficiently supply CPT, which is a starting compound of irinotecan hydrochloride and a variety of camptothecin derivatives, by a practical total synthesis, the invention provides a means of efficiently preparing a tricyclic ketone that corresponds to a CDE ring moiety of a camptothecin (CPT) skeleton.
参考文献:10.1055/s-0035-1561975 摘要:Han W, Jin F, Zhao Q, Du H, Yao L. Acid-Free Silver-Catalyzed Cross-Dehydrogenative Carbamoylation of Pyridines with Formamides. Synlett. 2016 Apr 06;27(12):1854–9. doi: 10.1055/s-0035-1561975.