专利号:US-2023278959-A1 优先权日:2020-05-04 标题:Synthesis of Optically Active Indoline Derivatives Via Ruthenium(II)-Catalyzed Enantioselective C-H Functionalization 发明人:CUI XIN; LI ZHONG-YUAN; CHAMINDA LAKMAL HETTI HANDI 权利人:UNIV MISSISSIPPI STATE 摘要:Provided herein are a method of Ru(II)-catalyzed enantioselective synthesis of a cyclic compound and cyclic compounds formed therefrom. The method includes providing a precursor compound having an unfunctionalized C—H bond and activating the unfunctionalized C—H bond by reacting the precursor compound in the presence of co-catalysts including a Ru(II) arene complex and a chiral transient directing group (CTDG).
专利号:US-2009234121-A1 优先权日:2008-01-16 标 题 :Tridentate (nnc) catalysts for the selective oxidation of hydrocarbons 发明人:PERIANA ROY A; GODDARD III WILLIAM A; OXGAARD JONAS; YOUNG KENNETH 权利人:PERIANA ROY A; GODDARD III WILLIAM A; OXGAARD JONAS; YOUNG KENNETH 摘要:The synthesis of discrete, air, protic, and thermally stable transition metal NNC complexes that catalyze the CH activation and functionalization of alkanes and arenes is disclosed. Methods for the selective conversion of methane to methanol or methyl esters in acidic and neutral media are disclosed.
专利号:US-8829238-B2 优先权日:2011-09-22 标 题:Methods for the synthesis of deuterated acrylate salts 发明人:YANG JUN; BONNESEN PETER V; HONG KUNLUN 权利人:YANG JUN; BONNESEN PETER V; HONG KUNLUN; UT BATTELLE LLC 摘要:A method for synthesizing a deuterated acrylate of the Formula (1), the method comprising: (i) deuterating a propiolate compound of Formula (2) to a methyne-deuterated propiolate compound of Formula (3) in the presence of a base and D 2 O: and (ii) reductively deuterating the methyne-deuterated propiolate compound of Formula (3) in a reaction solvent in the presence of deuterium gas and a palladium-containing catalyst to afford the deuterated acrylate of the Formula (1). The resulting deuterated acrylate compounds, derivatives thereof, and polymers derived therefrom are also described.
专利号:WO-2023033664-A1 优先权日:2021-09-04 标题:Cd44 glycoepitopes and chimeric vaccine glycoconjugates for cancer therapy and synthesis methods thereof 发明人:RIBEIRO DE CASTRO FERREIRA JOSÉ ALEXANDRE; MOREIRA NETO DA SILVA ANDRÉ; NEVES FREITAS RUI FILIPE; DE LARA SANTOS LÚCIO JOSÉ; RELVAS DOS SANTOS MARTA FILIPA; MILHAZES GAITEIRO CRISTIANA; FERREIRA PEIXOTO ANDREIA FILIPA; LINHARES MIRANDA ANDREIA RAFAELA; GOMES FERREIRA DYLAN; TEIXEIRA DE CASTRO FLÃ?VIA RAQUEL; CARMELINO CARDOSO SARMENTO BRUNO FILIPE; CARDOSO OLIVEIRA MARIA JOSÉ 权利人:I3S INSTITUTO DE INVESTIG E INOVACAO EM SAUDE ASSOCIACAO; INST PORTUGUES DE ONCOLOGIA DO PORTO FRANCISCO GENTIL EPE; REQUIMTE REDE DE QUIM E DE TECNOLOGIA ASSOCIACAO 摘要:The present invention refers to glycopeptides derived from the short CD44 isoforms lacking the amino acids encoded by exons 6-14, the said glycopeptides presenting at least one or multiple serine or threonine residues substituted with Tn ( GalNAca-O-Ser/Thr ) and/or sialyl-Tn (STn; Neu5Aca2-6GalNAca-O-Ser/Thr) antigens. The present invention further provides a method for synthesizing the herein disclosed glycopeptides, the said method comprising a one-pot glycosylation of synthetic short isoform CD44 peptides through combination with nucleotide sugars and glycosyl trans f erases and subsequent purification of the CD44s-Tn glycopeptides by lectin affinity chromatography followed by Ti02 chromatography or liquid chromatography. In one embodiment, the present invention further comprises immunogenic chimeras derived from the said CD44-Tn and/or STn glycopeptides, which are linked, in a polyvalent form, to a carrier immunogenic protein, such as keyhole limpet hemocyanin (KLH) or cross-reacting material (CRM197). Methods for conj ugating the synthesized CD44s-Tn glycopeptides to the immunogenic protein carriers CRM197 and KLH, are described, generating the chimeric glycopeptides, herein termed CRM197 -CD44 s-Tn and KLH-CD44s-Tn, respectively. The present invention further regards the above-mentioned CD44-Tn/STn glycopeptides or compositions comprising said glycopeptides for use in the treatment of cancer and pre-neoplastic diseases, most preferably of neoplastic diseases expressing short CD44 isoforms, through generation of antibodies against cancer cells and treatment and prevention of cancer by vaccination. The glycopeptides, compositions, synthesis methods and uses of the present invention can be advantageously employed in the treatment of cancer, alone or in combination with immune checkpoint inhibitor therapy, chemotherapy, and radiotherapy.
专利号:US-2023346952-A1 优先权日:2015-09-22 标题:Cannabinoid glycoside prodrugs and methods of synthesis 发明人:ZIPP BRANDON J; HARDMAN JANEE’ M; BROOKE ROBERT T; DEUTSCHER TYREL R 权利人:GRAPHIUM BIOSCIENCES INC 摘要:The present invention provides tetrahydrocannabinol glycoside and cannabidiol glycoside prodrugs and pharmaceutical compositions comprising these compounds, and their use for the site-specific delivery of tetrahydrocannabinol or cannabidiol. Also provided are processes for the preparation of purified tetrahydrocannabinol glycoside and cannabidiol glycoside prodrugs.
专利号:WO-2025008732-A1 优先权日:2023-07-03 标 题 :Novel compounds as modulators of il17 发明人:DESAI RANJIT; DESAI JIGAR 权利人:ZYDUS LIFESCIENCES LTD 摘要:The present invention relates to novel compounds of general formula (1), their suitable pharmaceutically acceptable salts, their solvates, their hydrates, their stereoisomers, their polymorphs, their racemic mixtures, their optically active forms and their use in the treatment of inflammatory conditions such as psoriasis, asthma, psoriatic arthritis or rheumatoid arthritis. Further, the present invention relates to processes of preparing such compounds, novel intermediates involved in their synthesis.
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