专利号:US-8188113-B2 优先权日:2006-09-14 标 题 :Dihydropyridopyrimidinyl, dihydronaphthyidinyl and related compounds useful as kinase inhibitors for the treatment of proliferative diseases 发明人:FLYNN DANIEL L; PETILLO PETER A; KAUFMAN MICHAEL D; PATT WILLIAM C 权利人:FLYNN DANIEL L; PETILLO PETER A; KAUFMAN MICHAEL D; PATT WILLIAM C; DECIPHERA PHARMACEUTICALS INC 摘要:The present invention relates to novel dihydropyridopyrimidinyl, dihydronaphthyridinyl, and related compounds which are kinase inhibitors and modulator useful for the treatment of various diseases. More particularly, the invention is concerned with such compounds, kinase/compound adducts, methods of treating diseases, and methods of synthesis of the compounds. Preferably, the compounds are useful for the modulation of kinase activity of Raf kinases and disease polymorphs thereof. Compounds of the present invention find utility in the treatment of mammalian cancers and especially human cancers including but not limited to malignant melanoma, colorectal cancer, ovarian cancer, papillary thyroid carcinoma, non small cell lung cancer, and mesothelioma. Compounds of the present invention also find utility in the treatment of rheumatoid arthritis and retinopathies including diabetic retinal neuropathy and macular degeneration.
专利号:US-2012245199-A1 优先权日:2009-12-23 标题:[4 [4-(aminomethyl-2-fluoro-phenyl)-piperidin-1-yl]-(1h-pyrrolo-pyridin-yl)-methanones and synthesis thereof 发明人:CHOI-SLEDESKI YONG MI; NIEDUZAK THADDEUS R; POLI GREGORY B; SHUM PATRICK WAI-KWOK; STOKLOSA GREGORY T; ZHAO ZHICHENG 权利人:CHOI-SLEDESKI YONG MI; NIEDUZAK THADDEUS R; POLI GREGORY B; SHUM PATRICK WAI-KWOK; STOKLOSA GREGORY T; ZHAO ZHICHENG; SANOFI SA 摘要:The present invention relates herein to compounds and compositions for the treatment and amelioration of inflammatory disease. Specifically the present invention relates to compounds that having a tryptase inhibition activity and the intermediates thereof, pharmaceutical compositions comprising such compounds, and a method of treating subjects suffering from a condition disease or disorder that can be ameliorated by the administration of an inhibitor of tryptase.
专利号:WO-2021078995-A1 优先权日:2019-10-25 标 题 :Selective polypeptide synthesis stalling assay and compound 发明人:STROUS GERARDUS JACOBUS ANTONIUS MARIA; MOL JAN ADRIANUS; VAN DER VELDEN LIEKE MARIE; KLUMPERMAN JUDITH; MAAS PETRUS EMMANUEL MARIE; PIET DENNIS PATRICK; DE KLERK-SPRENKELS NANDA ELISABETH; TIJHUIS JOHANN HEINRICH; VIÉTOR HENDRIK ENGELBERTUS; MAURICE MADELON MARIA; VAN DER KRIFT FELIX 权利人:UMC UTRECHT HOLDING BV; UNIV UTRECHT HOLDING BV; BIMINI BIOTECH B V 摘要:The invention relates to compounds, in particular pyrimidine-2,4-diamines, analogues and salts thereof and pharmaceutical compositions comprising pyrimidine-2,4-diamines analogues and salts thereof for use in the treatment and prevention of a disease, in particular a growth hormone receptor-dependent condition. The invention also relates to methods of using these compounds and compositions to treat physiological disorders related to the amount or activity of growth hormone. In a particular embodiment, the invention relates to a compound according to formula 1 for use in the treatment or prevention of a disease in a subject.
专利号:US-11767302-B2 优先权日:2020-10-01 标题 :Reagents and methods for tetrazine synthesis 发明人:FOX JOSEPH M; LAMBERT WILLIAM; FANG YINZHI; AM ENDE CHRISTOPHER WILLIAM; MAHAPATRA SUBHAM; XIE YIXIN; WANG CHUANQI 权利人:UNIV DELAWARE 摘要:Disclosed herein are mono- and di-substituted tetrazines and methods of their preparation and converting an oxetanyl ester to a thio-substituted tetrazine, which is then converted to a mono-substituted tetrazine, a di-substituted tetrazine, or a vinylether disubstituted tetrazine.
专利号:WO-2006079916-A1 优先权日:2005-01-26 标 题 :Thieno [2,3-d] pyrimidine compounds as inhibitors of adp-mediated platelets aggregation 发明人:ENNIS MICHAEL DALTON; KORTUM STEVEN WADE; RAHMAN HAYAT; SCHWEITZER BARBARA ANN; TENBRINK RUTH ELIZABETH 权利人:PHARMACIA & UPJOHN CO LLC; ENNIS MICHAEL DALTON; KORTUM STEVEN WADE; RAHMAN HAYAT; SCHWEITZER BARBARA ANN; TENBRINK RUTH ELIZABETH 摘要:Compounds and pharmaceutically acceptable salts of the compounds are disclosed, wherein the compounds have the structure of Formula (I): wherein A1, A2, A3, A4, A5, A6, A7, A8, X4, X6, R2, R4, R5, and R6 are as defined in the detailed description of the invention. Corresponding pharmaceutical compositions, methods of treatment, methods of synthesis, and intermediates are also disclosed.
专利号:US-2009227575-A1 优先权日:2008-03-04 标 题 :7H-PYRROLO[2,3-H]QUINAZOLINE COMPOUNDS, THEIR USE AS mTOR KINASE AND PI3 KINASE INHIBITORS, AND THEIR SYNTHESIS 发明人:VENKATESAN ARANAPAKAM MUDUMBAI; CHEN ZECHENG; DOS SANTOS OSVALDO; BROOIJMANS NATASJA; GOPALSAMY ARIAMALA 权利人:WYETH CORP 摘要:A 7H-pyrrolo[2,3-h]quinazoline compound of the formula I n n n n n n n n n n wherein Ar, R 1 , R 2 , R 7 , R 8 , R 9 , R 10 , R 11 , R 12 , and n are as defined in the specification, and methods for making same.