专利号:WO-2024182268-A1 优先权日:2023-02-27 标 题 :Liquid phase peptide support synthesis of peptides and peptidomimetics 发明人:HAN AMY 权利人:REGENERON PHARMA 摘要:The present invention provides compounds useful as support for liquid phase organic synthesis e.g., liquid phase organic synthesis of peptides and peptidomimetics. In one aspect, the present invention provides a compound having a structure of Formula (I) where R1, R2, R3, m, and n are as described herein and methods of making and using same.
专利号:US-11897914-B2 优先权日:2021-11-29 标题 :Synthesis of 2′ protected nucleosides 发明人:POON WING C; ZOU RUIMING; LAU ALDRICH N K; YU DAVID; Du Gengyu; YAO YUN-CHIAO; ZHAO GANG 权利人:HONGENE BIOTECH CORP 摘要:Embodiments of the present application relate to the preparation of 2′-O-protected nucleoside phosphoramidites and conjugation of the 2′-O-protected nucleoside to a solid support. More specifically, the present application relates to nucleosides having a hydroxy protecting group at the 2′ position that reduces migration to the 3′ position during RNA (e.g., mRNA) synthesis and can be readily removed under mild conditions without the use of toxic metal-containing reagents. Methods of using the nucleosides described herein in RNA synthesis are also disclosed.
专利号:US-6172226-B1 优先权日:1993-12-22 标 题:Synthons for the synthesis and deprotection of peptide nucleic acids under mild conditions 发明人:COULL JAMES M; EGHOLM MICHAEL; HODGE RICHARD P; ISMAIL MOHAMED; RAJUR S B 权利人:PERSEPTIVE BIOSYSTEMS INC 摘要:A method is disclosed for preparing novel PNA synthons having protecting groups capable of removal under mild conditions. The PNA synthons are prepared by coupling novel N-substituted nucleobase intermediates having carbamate protection of the exocyclic amino group of the heterocycle to an amino protected backbone or an amino protected backbone ester of the amino acid N-(2-aminoethyl)-glycine. By the method of this invention, the resultant PNA synthons can have orthogonal protection of the carbamate protected nucleobase and the amino protected backbone. The PNA synthons are useful in the synthesis of peptide nucleic acids (PNAs) and other oligomers such as PNA-DNA chimeras, and may be used in automated synthesizers. Novel compositions of matter are also disclosed. In addition, a guanine PNA synthon having selective carbamate protection of the exocyclic 2-amino group with the C6 carbonyl group unprotected is disclosed.
专利号:US-6951878-B2 优先权日:1998-03-12 标 题:Benzo[b]thiophenyl or tetrahydro-benzo[b]thiophenyl modulators of protein tyrosine phosphatases (PTPases) 发明人:MOELLER NIELS PETER HUNDAHL; ANDERSEN HENRIK SUNE; IVERSEN LARS FOGH; OLSEN OLE HVILSTED; BRANNER SVEN; HOLSWORTH DANIEL DALE; BAKIR FARID; JUDGE LUKE MILBURN; AXE FRANK URBAN; JONES TODD KEVIN; RIPKA WILLIAM CHARLES; GE YU; UYEDA ROY TERUYUKI 权利人:NOVO NORDISK AS 摘要:The present invention provides novel compounds, novel compositions, methods of their use, and methods of their manufacture, where such compounds are pharmacologically useful inhibitors of Protein Tyrosine Phosphatases (PTPase's) such as PTP1B, CD45, SHP-1, SHP-2, PTPα, LAR and HePTP or the like. n The compounds are useful in the treatment of type I diabetes, type II diabetes, impaired glucose tolerance, insulin resistance, obesity, immune dysfunctions including autoimmunity diseases with dysfunctions of the coagulation system, allergic diseases including asthma, osteoporosis, proliferative disorders including cancer and psoriasis, diseases with decreased or increased synthesis or effects of growth hormone, diseases with decreased or increased synthesis of hormones or cytokines that regulate the release of/or response to growth hormone, diseases of the brain including Alzheimer's disease and schizophrenia, and infectious diseases.
专利号:US-4894385-A 优先权日:1985-01-16 标 题:Imidazole derivatives as inhibitors of TXA2 synthesis 发明人:KAWAMOTO ISAO; ENDO ROKURO; MATSUDA KEIICHI; USHIYAMA SHIGERU; OSHIMA TAKESHI 权利人:SANKYO CO 摘要:Compounds of formula (I): ##STR1## (wherein n is 0, 1 or 2 and R 1 , R 2 , R 4 , R 5 , R 6 , X, Y and Z are a variety of groups and atoms) have the ability to inhibit the synthesis of thromboxane A 2 and hence are useful in the treatment or prophylaxis of thrombotic conditions.
专利号:US-8653238-B2 优先权日:2006-02-27 标题:Compositions and methods for transport of molecules with enhanced release properties across biological barriers 发明人:WENDER PAUL A; GOUN ELENA A; JONES LISA R 权利人:WENDER PAUL A; GOUN ELENA A; JONES LISA R; UNIV LELAND STANFORD JUNIOR 摘要:Conjugates of a cargo molecule with a transporter molecule are disclosed, where the cargo molecule and the transporter molecule are linked covalently by a releasable linker. The cargo of the conjugate can be a biologically active agent or a reporter molecule. The transporter modulates the transport of the cargo across a biological barrier (e.g., a cell membrane) compared to the transport of the unconjugated cargo. Releasable linkers suitable for rapid and facile conjugation to various types of cargo and transporters are also disclosed, along with methods for using the linkers in the synthesis of conjugates.
[参考文献]: D A Bennett, Et Al. Mechanism Of Sulfide Oxidations By Peroxymonocarbonate. Inorg Chem. 2001 Jun 18;40(13):2996-3001.
合成参考文献
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