专利号:WO-2011110511-A1 优先权日:2010-03-11 标题:Spect imaging agents of amyloid plaques 发明人:SCHMITT-WILLICH HERIBERT; HEINRICH TOBIAS; BROCKSCHNIEDER DAMIAN 权利人:Bayer Pharma AG; SCHMITT-WILLICH HERIBERT; HEINRICH TOBIAS; BROCKSCHNIEDER DAMIAN 摘要:The invention relates to novel iodine -radiolabeled compounds useful for diagnosing Alzheimer's desease, to respective novel precursors for the synthesis of such compounds, and to the process of manufacturing said imaging agent of the following Formula (I), wherein Q is a six membered aromatic ring, either carbocycle or heterocycle with one N- atom, wherein X 1 , X 2 , X 3 , X 4 and X 5 are independently selected from N or C, and wherein zero or one of X 1 ( X 2 , X 3 , X 4 or X 5 is N and the remaining ones are C; A is either Sn(alkyl)3, I, l-123, l-124, l-125, l-131, Br; wherein alkyl comprises methyl, ethyl, propyl, butyl, pentyl and hexyl, Y is C or N; with the proviso that if X 1 ( X 2 , X 3 , X 4 or X 5 has the meaning of N, substitution by A in that position is excluded; or a pharmaceutically acceptable salt thereof.
专利号:US-8598166-B2 优先权日:2008-03-21 标 题:Polysubstituted derivatives of 6-heteroarylimidazo[1,2-a]pyridines, and preparation and therapeutic use thereof 发明人:DE PERETTI DANIELLE; EVANNO YANNICK; MACHNIK DAVID; RAKOTOARISOA NATHALIE 权利人:DE PERETTI DANIELLE; EVANNO YANNICK; MACHNIK DAVID; RAKOTOARISOA NATHALIE; SANOFI SA 摘要:Compounds of formula (I): n nwherein R 1 , R 2 , R 3 , R 4 , Het and X are as defined in the disclosure, or an acid addition salt thereof, and the therapeutic use and process of synthesis thereof.
专利号:US-2010004245-A1 优先权日:2006-10-20 标 题:Azacycloalkane derivatives as inhibitors of stearoyl-coenzyme a delta-9 desaturase 发明人:OBALLA RENATA M; DESCHENES DENIS; GAGNON MARC; LEBLANC YVES; POWELL DAVID; RAMTOHUL YEEMAN K 权利人:MERCK FROSST CANADA LTD 摘要:Azacycloalkane derivatives of structural formula (I) are selective inhibitors of stearoyl-coenzyme A delta-9 desaturase (SCD1) relative to other known stearoyl-coenzyme A desaturases. The compounds of the present invention are useful for the prevention and treatment of conditions related to abnormal lipid synthesis and metabolism, including cardiovascular disease, such as atherosclerosis; obesity; diabetes; neurological disease; metabolic syndrome; insulin resistance; and liver steatosis.
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:WO-2011095593-A1 优先权日:2010-02-08 标 题 :Iodo precursor for a pet imaging agent of amyloid plaques 发明人:SCHMITT-WILLICH HERIBERT; HEINRICH TOBIAS; BROCKSCHNIEDER DAMIAN 权利人:BAYER SCHERING PHARMA AG; SCHMITT-WILLICH HERIBERT; HEINRICH TOBIAS; BROCKSCHNIEDER DAMIAN 摘要:The invention relates to a precursor for a [ 18 F]-labeled PET tracer for imaging of Alzheimer's Disease, its synthesis and the process for preparing the respective [ 18 F]-labeled PET tracer.
专利号:CN-114213236-A 优先权日:2021-11-30 标 题:Synthesis of Yeast Dehydrogenase Inhibitor
参考标题:Synthesis And Characterization Of A Series Of Bis-Homoleptic Cycloruthenates With Terdentate Ligands As A Family Of Panchromatic Dyes 作者:Thomas W. Rees,Jinfeng Liao,Alessandro Sinopoli,Louise Male,Giuseppe Calogero,Basile F.E. Curchod,Etienne Baranoff |发布日期:2017.8.21 摘要:A Series Of Six Homoleptic Bis-Cyclometalated Ruthenium Complexes, Ru(N^n^c)2, Is Reported Where N^n^c Is A 6-(2,4-Difluoro-3-R3-Phenyl)-4-R2-4′-R1-2,2′-Bipyridine With R3 = −h Or −cf3 And R2 And R1 = −cooet Or −cf3. An Effective Synthesis Of The Ligands And The Complexes Is Described. The Uv-Visible Absorption Studies Demonstrate That These Complexes Are Panchromatic Dyes Absorbing Up To 900 Nm. Importantly