CAS: 1038915-60-4; (S)-2-(4-(Piperidin-3-yl)Phenyl)-2H-Indazole-7-Carboxamide

上下游产品

racemic 3-{4-[7-(amin°Carbonyl)-2H-indazol-2-yl]phenyl}piperidinium chloride tert-butyl 3-[4-({[3-(methoxycarbonyl)-2-nitrophenyl]methylene}amino)phenyl]piperidine-1-carboxylate methyl 2-{4-[1-(tert-butoxycarbonyl)piperidin-3-yl]phenyl}-2H-indazole-7-carboxylate 3-methyl-2-nitrobenzoic acid(3S)-3-[4-[7-(amin°Carbonyl)-2H-indazol-2-yl]phenyl]piperidinium chloride 2-[4-((3S)-3-piperidinyl)phenyl]-2H-indazole-7-carboxamide p-toluenesulfonic acid salt

Niraparib置于n-乙酰-L-亮氨酸体系中,用 甲醇 用作溶剂,化学反应 1.0H,以91.2%的收率获得尼拉帕尼
参考文献:一种制备niraparib的合成方法
标题:一种制备niraparib的合成方法
摘要:一种制备niraparib的合成方法,该方法包括起始原料3‑甲基‑2‑硝基苯甲酸经酯化,3位甲基醛化,席夫碱反应,环化,酰胺化,脱b°C,手性拆分得到纯度达到91%以上的光学纯niraparib.本发明方法简便,效率高,易于操作,设备要求少,是一种适合工业化生产的方法.

专利信息

专利号:WO-2022238500-A1
优先权日:2021-05-12
标题 :Radiosynthesis of [18f] talazoparib
发明人：BOWDEN GREGORY DAVID; MAURER ANDREAS; STOTZ SOPHIE; KINZLER PAUL JOHANNES OSKAR MARIA; LAEMMERHOFER MICHAEL; ZENDER LARS; PICHLER BERND
权利人:UNIV TUEBINGEN MEDIZINISCHE FAKULTAET
摘要:The present invention relates to the synthesis of Poly (ADP ribose) polymerase (PARP) inhibitors and particularly to the radiosynthesis of PARP 1 inhibitors, more particularly to the synthesis of [18F] talazoparib.

专利号:US-12043612-B2
优先权日:2020-05-09
标 题 :Methods of manufacturing a bifunctional compound, ultrapure forms of the bifunctional compound, and dosage forms comprising the same
发明人：ALLAN LAURA E N; CHEN CHUNGPIN HERMAN; DONG HANQING; GROSSO JOHN A; HASKELL III ROYAL J; LLOYD RHYS; REECE HAYLEY
权利人:ARVINAS OPERATIONS INC
摘要:The present disclosure relates to ultra-pure forms, polymorphs, amorphous forms, and formulations of N-[(1r,4r)-4-(3-chloro-4-cyanophenoxy)cyclohexyl]-6-[4-({4-[2-(2,6-dioxopiperidin-3-yl)-6-fluoro-1,3-dioxo-2,3-dihydro-1H-isoindol-5-yl]piperazin-1-yl}methyl)piperidin-1-yl]pyridazine-3-carboxamide, referred to herein as Compound A:The present disclosure also relates methods of manufacturing and purifying the same, as well as intermediates useful in the synthesis of Compound A. The ultra-pure forms, polymorphs, amorphous forms, and formulations of Compound A can be used as therapeutic agents for the treatment of various diseases and conditions such as cancer.

专利号:US-10927095-B2
优先权日:2017-08-14
标 题:Processes for the preparation of Niraparib and intermediates thereof
发明人：LUTHRA PARVEN K; VASOYA SANJAY L; PATIL BHATU T; TANEJA AMIT K; SRIVASTAV NAVEEN C; SINGH RINKU
权利人:TEVA PHARMACEUTICALS INT GMBH
摘要:The present invention relates to novel procedures and novel intermediates useful in the synthesis of Niraparib or any salt thereof.

专利号:US-11629137-B2
优先权日:2017-04-24
标 题:Methods of manufacturing of niraparib
发明人：STEWART ALISTAIR; TOTO ANTHONY JOSEPH; CHEN FRANK XING; WU GEORGE
权利人:TESARO INC
摘要:Disclosed herein are methods and processes of preparing niraparib and pharmaceutically acceptable salts thereof, and intermediates and their salts useful for the synthesis of niraparib.

专利号:US-11801232-B2
优先权日:2019-11-27
标 题 :Targeting of ARID1A-deficient cancers by inhibiting de novo pyrimidine synthesis pathway
发明人：HUANG GLORIA
权利人:UNIV YALE
摘要:This application relates to methods and kits for treating ARID1A-mutant tumors, cancers, or aberrantly proliferating cells and subjects harboring the tumors, cancers, or aberrantly proliferating cells. In particular, the methods provided include administering to the subject or cell an effective amount of a pyrimidine synthesis inhibitor and administering to the subject or cell an effective amount of a DNA repair inhibitor. The kits include a) a composition comprising a pyrimidine synthesis inhibitor and b) a composition comprising a DNA repair inhibitor.

专利号:US-9993570-B2
优先权日:2014-01-05
标题:Radiolabeled tracers for poly (ADP-ribose) polymerase-1 (PARP-1), methods and uses therefor
发明人：MACH ROBERT; CHU WENHUA; ZHOU DONG; MICHEL LOREN; CHEN DELPHINE
权利人:UNIV WASHINGTON
摘要:Disclosed are PARP-1 inhibitors, which can be 18 F-labeled for use as tracers in positron emission tomographic (PET) imaging. Further disclosed are methods of synthesis. Of the compounds synthesized, 2-[p-(2-Fluoroethoxy)phenyl]-1.3.10-triazatricyclo[6.4.1.0 4,13 ]trideca-2,4(13),5,7-tetraen-9-one (12) had the highest inhibition potency for PARP-1 (IC 50 =6.3 nM). Synthesis of [ 18 F]-12 is disclosed under conventional conditions in high specific activity with 40-50% decay-corrected yield. MicroPET imaging using [ 18 F]-12 in MDA-MB-436 tumor-bearing mice demonstrated accumulation of [ 18 F]-12 in a tumor. Binding, can be blocked by olaparib. The compounds have utility for tumor imaging.