专利号:US-8546532-B2 优先权日:2008-04-17 标题:Synthesis of directed sequence polymer compositions and antibodies thereof for the treatment of protein conformational disorders 发明人:BONNIN DUSTAN; ZANELLI ERIC; MATHERS THOMAS 权利人:BONNIN DUSTAN; ZANELLI ERIC; MATHERS THOMAS; DECLION PHARMACEUTICALS INC 摘要:The instant invention comprises a process for the solid phase synthesis of directed epitope peptide mixtures useful in the treatment and diagnosis of protein conformational disorders, such process defined by a set of rules regarding the identity and the frequency of occurrence of amino acids that substitute a base or native amino acid of a known epitope. The resulting composition is a mixture of related peptides for therapeutic use. The invention also pertains to the process of generating antibodies using the directed epitope peptide mixtures as the antigens, and antibodies generated by such process, useful in the treatment and diagnostics of the said protein conformational disorder.
专利号:US-4879389-A 优先权日:1986-06-25 标题:Chiral phosphinopyrrolidine compounds and their use for asymmetric synthesis of optically active compounds 发明人:ACHIWA KAZUO 权利人:ACHIWA KAZUO 摘要:New chiral phosphinopyrrolidine compounds of the general formula: (I) or (I') wherein R1 is a hydrogen atom, -COR, -COOR, -CONHR or -SO2-R where R is an alkyl or aryl group, R2 and R3 each represents independently an aryl group which may have a substituent or substituents, and R4 and R5 each represents independently an aliphatic or cycloaliphatic hydrocarbyl group which may have a substituent or substituents, as well as the use of these compounds as ligand for a metal complex catalyst for asymmetric synthesis of optically active compounds. The new chiral phosphinopyrrolidine compounds are useful ligands which attain both of high optical yield and high reaction efficiency in catalytic asymmetric reduction.
专利号:US-8202985-B2 优先权日:2005-10-31 标 题:Monomer compositions for the synthesis of polynucleotides, methods of synthesis, and methods of deprotection 发明人:DELLINGER DOUGLAS J; TIMAR ZOLTAN; SIERZCHALA AGNIESZKA; DELLINGER GERALDINO; CARUTHERS MARVIN H 权利人:DELLINGER DOUGLAS J; TIMAR ZOLTAN; SIERZCHALA AGNIESZKA; DELLINGER GERALDINO; CARUTHERS MARVIN H; AGILENT TECHNOLOGIES INC; UNIV COLORADO 摘要:Nucleotide monomers, polynucleotides, methods of making each, and methods of deprotecting each, are disclosed. An embodiment of the nucleotide monomer, among others, includes a nucleotide monomer having a heterobase protecting group selected from structures I through III as described herein. An embodiment of the polynucleotide, among others, includes a plurality of nucleotide moieties having a heterobase protecting group selected from one of structures I through III as described herein.
专利号:US-7759471-B2 优先权日:2005-10-31 标题 :Monomer compositions for the synthesis of RNA, methods of synthesis, and methods of deprotection 发明人:DELLINGER DOUGLAS J; TIMAR ZOLTAN; SIERZCHALA AGNIESZKA; DELLINGER GERALDINE; CARUTHERS MARVIN H 权利人:AGILENT TECHNOLOGIES INC; UNIV COLORADO 摘要:Nucleotide monomers, polynucleotides, methods of making each, methods of deprotecting each, and the like are disclosed herein.
专利号:US-9051302-B2 优先权日:2008-01-15 标 题 :Synthesis of resorcylic acid lactones useful as therapeutic agents 发明人:WINSSINGER NICOLAS; BARLUENGA SOFIA; KARPLUS MARTIN 权利人:WINSSINGER NICOLAS; BARLUENGA SOFIA; KARPLUS MARTIN; UNIV STRASBOURG 摘要:Disclosed are macrocyclic compounds of formulae I, I′, II, II′, III, III′, IV, and V, which are analogs of the pochonin resorcylic acid lactones, pharmaceutical compositions comprising the compounds, and methods and uses comprising the compounds for the treatment of diseases mediated by kinases and Heat Shock Protein 90 HSP90.
专利号:US-2024287041-A1 优先权日:2021-05-20 标题 :Methods of synthesis of heteroaryl derivatives of triazolyl acrylamides and crystalline forms 发明人:BALOGLU ERKAN; AUSTAD BRIAN C; ROE DAVID G; KEDUC ANDREW; GOTTSCHLING STEPHEN EDMUND; HECKER EVAN 权利人:KARYOPHARM THERAPEUTICS INC 摘要:The present invention relates to a method of preparing a compound represented by structural formula (VII), comprising reacting a compound represented by structural formula (II), with a compound represented by structural formula (III), in a solvent, in the presence of a Pd catalyst and one or more inorganic bases under conditions suitable to prepare a compound represented by structural formula (VII): The values and example values of the variables in structural formulas (VII), (II), and (III) are defined herein. The present invention also relates to crystalline Forms I and II of the compound represented by Structural Formula (VII), the use of the crystalline Forms in treating disease or disorders associated with CRM1 and method of preparing the crystalline Forms.