专利号:US-7138526-B1 优先权日:1999-06-15 标 题 :Solid phase synthesis of n,n-disubstituted diazacycloalkylcarboxy derivatives 发明人:HERPIN TIMOTHY F; MORTON GEORGE C; SALVINO JOSEPH M 权利人:AVENTIS PHARMA INC 摘要:A method for the solid phase synthesis of N,N-disubstituted diazacycloalkylcarboxy derivatives of general formula (I) and (II) is claimed. Examples include piperazine-2-carboxamide. The method is applicable to the synthesis or large combinatorial libraries
专利号:US-7897762-B2 优先权日:2006-09-14 标 题:Kinase inhibitors useful for the treatment of proliferative diseases 发明人:FLYNN DANIEL L; PETILLO PETER A; KAUFMAN MICHAEL D; PATT WILLIAM C 权利人:DECIPHERA PHARMACEUTICALS LLC 摘要:The present invention relates to novel kinase inhibitors and modulator compounds 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-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:WO-9700244-A1 优先权日:1995-06-19 标题 :Process for parallel synthesis of a non-peptide library 发明人:FRITZ JAMES E; KALDOR STEPHEN W 权利人:LILLY CO ELI; FRITZ JAMES E; KALDOR STEPHEN W 摘要:A process for the sequential preparation of a library of compounds having pharmaceutical usage. The process involves the sequential mixing of solution phase reagents, followed by scavenging of excess unreacted reagents with solid phase scavenging agents. The process is highly iterative and applicable for producing various ureas, thiureas, amides, carbonates and tertiary amines.
专利号:US-10385167-B2 优先权日:2015-02-13 标题:Process for the synthesis of polyoxazolidinone compounds with high stability 发明人:MÜLLER THOMAS ERNST; Gürtler Christoph; BASU SUSMIT; RANGHEARD CLAUDINE; RIVILLO DAVID; LEITNER WALTER; Köhler Burkhard 权利人:COVESTRO DEUTSCHLAND AG 摘要:The present invention relates to polyoxazolidinone compounds, a method for the production of polyoxazolidinone compounds, comprising the step of reacting a biscarbamate compound with a bisepoxide compound in the presence of a mono-carbamate, a mono-isocyanate and/or a mono-epoxide compound as chain regulator and a suitable base having a pK b value of ≤9 as catalyst. The invention further relates to the use of polyoxazolidinone compounds with high thermal stability.
专利号:US-11326018-B2 优先权日:2016-08-19 标 题:Process for the synthesis of polyoxazolidinone compounds 发明人:WEBER ANNA; RANGHEARD CLAUDINE; KESSLER MICHAEL; LEITNER WALTER; Gürtler Christoph; KOOPMANS CARSTEN; MÜLLER THOMAS ERNST 权利人:COVESTRO DEUTSCHLAND AG 摘要:A method for the production of polyoxazolidinone compounds, comprising the step of reacting an isocyanate compound (A) with an epoxide compound (B) in the presence of a catalyst (C), wherein the isocyanate compound (A) comprises a isocyanate compound (A 1 ) wherein the a isocyanate compound (A1) comprising at least two isocyanate groups (I 1 ≥2), preferred two isocyanate groups (I 1 =2), wherein the epoxide compound (B) comprises a epoxide compound (B 1 ) and an epoxide compound (B 2 ), wherein the epoxide compound (B 2 ) is different from the epoxide compound (B 1 ) wherein the epoxide compound (B 1 ) comprising at least two terminal epoxide groups (F1≥2), preferred two terminal epoxide groups (F 1 =2), linked together by a linking group (L1) and the epoxide compound (B 2 ) comprising at least two terminal epoxide groups (F 2 ≥2)), preferred two terminal epoxide groups (F 2 =2), linked together by a linking group (L 2 ), wherein the linking group (L 2 ) comprises acyclic and covalent bonds to each other free of conjugated multiple bonds within the main chain, wherein the epoxide compound (B 2 ) is present in the epoxide compounds B 1 and B 2 , in an amount of ≥0.01 mol-% to <10 mol-%, preferred 1-9 mol-% more preferred 3-8 mol-% based on the molar ratio the terminal epoxide groups in the epoxide compound (B 1 ) and of the sum of the terminal epoxide groups in the epoxide compound (B 1 ) and terminal epoxide groups in the epoxide compound (B 2 ).