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-5174980-A 优先权日:1991-10-04 标题 :Synthesis of crystalline ZSM-35 发明人:HELLRING STUART D; STRIEBEL RANDY F 权利人:MOBIL OIL CORP 摘要:This invention relates to a new form of crystalline material identified as having the structure of ZSM-35, to a new and useful method for synthesizing said crystalline material and to use of said crystalline material prepared in accordance herewith as a catalyst for organic compound, e.g. hydrocarbon compound, conversion.
专利号:US-8003785-B2 优先权日:2008-06-18 标 题 :Halo-substituted pyrimidodiazepines 发明人:CAI JIANPING; CHEN SHAOQING; CHU XIN-JIE; LUK KIN-CHUN; MISCHKE STEVEN GREGORY; SUN HONGMAO; WOVKULICH PETER MICHAEL 权利人:TAKEDA PHARMACEUTICAL 摘要:The present invention provides PLK1 inhibitor compounds of formula I: n nuseful in the treatment or control of cell proliferative disorders, particularly oncological disorders. These compounds and formulations containing such compounds may be useful in the treatment or control of solid tumors, such as, for example, breast, colon, lung and prostate tumors and other oncological diseases such as non-Hodgkin's lymphomas. Also provided are intermediate compounds useful in the synthesis of compounds of formula I.
专利号:US-7615634-B2 优先权日:2003-02-10 标题:4-aminopyrimidine-5-one derivatives 发明人:BARTKOVITZ DAVID JOSEPH; CHU XIN-JIE; DING QINGJIE; JIANG NAN; LOVEY ALLEN JOHN; MOLITERNI JOHN ANTHONY; MULLIN JR JOHN GUILFOYLE; VU BINH THANH; WOVKULICH PETER MICHAEL 权利人:HOFFMANN LA ROCHE 摘要:Novel intermediate compounds are disclosed. These compounds are useful in the synthesis of 4-aminopyrimidine-5-one derivatives that inhibit cyclin-dependent kinases, in particular cyclin-dependent kinase 4 (Cdk4). The 4-aminopyrimidine-5-one derivatives and their pharmaceutically acceptable salts have antiproliferative activity and are useful in the treatment or control of cancer, in particular solid tumors.
专利号:US-2023025807-A1 优先权日:2019-10-30 标题:Cd38 inhibitors 发明人:KULKARNI SANTOSH S; LAGU BHARAT; WU XINYUAN 权利人:MITOBRIDGE INC 摘要:The present invention is directed to a compound of Formula (I) or a pharmaceutically acceptable salt thereof. Compounds of Formula (I) are CD38 inhibitors, which can be used to treat a disease or condition in a subject that benefits from an increase in NAD + or to treat a mitochondrial disorder in a subject. Such disease or condition is a muscle structure disorder, a neuronal activation disorder, a muscle fatigue disorder, a muscle mass disorder, a metabolic disease, a cancer, a vascular disease, an ocular vascular disease, a muscular eye disease, or a renal disease. The present description discloses the synthesis and characterisation of exemplary compounds as well as pharmacological data thereof (e.g. pages 30 to 135; examples 1 to 61; table). Such an exemplary compound is e.g. N-((1r,4r)-4-(2-methoxyethoxy) cyclohexyl)-5-(thiazol-5-yl)-1H-indole-7-carboxamide (II).
专利号:US-7388112-B2 优先权日:2003-05-23 标题 :Immunomodulation with novel pharmaceutical compositions 发明人:BURNS MARK R; MCVEAN MARALEE; KENNEDY KEVIN; YEUNG ARTHUR; DEVENS BRUCE H 权利人:MEDIQUEST THERAPEUTICS INC 摘要:The synthesis and use of a novel class of tumor necrosis factor (TNFα) inhibitors and immunomodulators are provided. Examples are those having the structures: n nwherein a, b and c are integers from 0 to 12, X equals NH or CHNH 2 , R 1 and R 2 each is a hydrogen or a C 1 to C 20 aliphatic; aliphatic amine; an alicyclic; aromatic; heterocycle; and halogenated forms thereof; andn n n n n n n n n n n n n wherein, a, b and c are integers from 0 to 12; R 1 , R 2 , R 3 , and R 4 each is a hydrogen or a C 1 to C 20 ; aliphatic amine; an alicyclic; aromatic; a heterocycle; and halogenated forms thereof.
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