专利号:US-2008031812-A1 优先权日:1999-06-02 标 题:Redox-stable, non-phosphorylated cyclic peptide inhibitors of sh2 domain binding to target protein, conjugates, thereof, compositions and methods of synthesis and use 发明人:ROLLER PETER P; LONG YA-QIU; LUNG FENG-DI T; KING C RICHTER; YANG DAJUN; VOIGT JOHANNES H 权利人:GOVERNMENT OF THE USA REPRESEN; UNIV GEORGETOWN 摘要:A compound of formula: n n nin which (i) aa 1 is Adi and aa 4 is Glu or (ii) each of aa 1 and aa 4 is Adi, L is sulfur, sulfoxide, oxygen or methylene, which compound (and its conjugates) bind to an SH2 domain in a protein comprising an SH2 domain, is non-phosphorylated, is redox-stable in vivo, is characterized by an IC 50 in vivo of less than about 4.0 μM with respect to the SH2 domain in Grb2, and, upon binding to the SH2 domain of Grb2, has a turn conformation. A conjugate comprising a compound as described above and a carrier agent, a composition comprising (i) a compound or a conjugate as described above and (ii) a carrier, a method of inhibiting binding of an SH2 domain in a protein comprising an SH2 domain to a target protein in an animal, wherein the SH2 domain is contacted with a target protein-binding inhibiting effective amount of a compound or a conjugate as described above, and a method of synthesizing such conjugates.
专利号:US-8734846-B2 优先权日:2008-06-16 标 题 :Methods for the preparation of targeting agent functionalized diblock copolymers for use in fabrication of therapeutic targeted nanoparticles 发明人:ALI MIR M; HRKACH JEFF; ZALE STEPHEN E; ALVAREZ DE CIENFUEGOS LUIS 权利人:BIND BIOSCIENCES INC 摘要:This application provides nanoparticles and methods of making nanoparticles using pre-functionalized poly(ethylene glycol)(also referred to as PEG) as a macroinitiator for the synthesis of diblock copolymers. Ring opening polymerization yields the desired poly(ester)-poly (ethylene glycol)-targeting agent polymer that is used to impart targeting capability to therapeutic nanoparticles. This “polymerization fromâ€? approach typically employs precursors of the targeting agent wherein the reactivity of functional groups of the targeting agent is masked using protecting groups. Also described is a “coupling toâ€? that utilized the poly(ethylene glycol)-targeting agent conjugate where the targeting agent remains in its native un-protected form. This method uses “orthogonalâ€? chemistry that exhibit no cross reactivity towards functional groups typically found within targeting agents of interest.
专利号:US-8759632-B2 优先权日:2005-07-05 标 题 :Polynucleotides encoding isoprenoid modifying enzymes and methods of use thereof 发明人:RO DAE-KYUN; NEWMAN KARYN; PARADISE ERIC M; KEASLING JAY D; OUELLET MARIO; EACHUS RACHEL; HO KIMBERLY; HAM TIMOTHY 权利人:RO DAE-KYUN; NEWMAN KARYN; PARADISE ERIC M; KEASLING JAY D; OUELLET MARIO; EACHUS RACHEL; HO KIMBERLY; HAM TIMOTHY; UNIV CALIFORNIA 摘要:The present invention provides isolated nucleic acids comprising nucleotide sequences encoding isoprenoid modifying enzymes, as well as recombinant vectors comprising the nucleic acids. The present invention further provides genetically modified host cells comprising a subject nucleic acid or recombinant vector. The present invention further provides a transgenic plant comprising a subject nucleic acid. The present invention further provides methods of producing an isoprenoid compound, the method generally involving culturing a subject genetically modified host cell under conditions that permit synthesis of an isoprenoid compound modifying enzyme encoded by a subject nucleic acid.
专利号:US-2013035307-A1 优先权日:2010-01-26 标 题:Methods for treating or preventing the spread of cancer using semi-synthetic glycosaminoglycosan ethers 发明人:PRESTWICH GLENN D; KENNEDY THOMAS P 权利人:UNIV UTAH RES FOUND; PRESTWICH GLENN D; KENNEDY THOMAS P 摘要:Described herein are methods for the treatment and prevention of tumor metastasis using alkylated and fluoroalkylated semi-synthetic glycosaminoglycan ethers (“SAGEsâ€?). The synthesis of sulfated alkylated and fluoroalkylated SAGEs is also described.
专利号:US-2008214827-A1 优先权日:2004-02-03 标 题:Synthesis of Cyanoimino-Benzoimidazoles 发明人:GOEHRING R RICHARD; WHITEHEAD JOHN; SHAO BIN 权利人:EURO CELTIQUE SA 摘要:Disclosed in certain embodiments is a process for synthesizing a compound of formula (V) and salts thereof.
专利号:WO-2005079742-A1 优先权日:2004-02-19 标 题:Cosmetic and/or dermatological agent for increasing the endogenous lipid content of the skin 发明人:VEEGER MARCEL; KLOTZ ANDREAS; ZUR MUEHLEN ANNETTE; THOERNER BRIGITTE 权利人:STOCKHAUSEN CHEM FAB GMBH; VEEGER MARCEL; KLOTZ ANDREAS; ZUR MUEHLEN ANNETTE; THOERNER BRIGITTE 摘要:The invention relates to the use of at least one active ingredient that is selected from the water-soluble groups: (a) allantoin; (b) salts and/or esters of gluconic acid and/or aspartic acid; (c) precursors of creatine, creatine and creatinine and their derivatives; (d) glycyrrhetinic acid or the salts and/or esters thereof; (e) D-panthenol and/or at least one active ingredient that is selected from the oil-soluble groups: (f) vitamin E acetate; (g) cholesterol; (h) derivatives of glycyrrhetinic acid, in so far as they are soluble in the oils and fats that are conventionally used in the cosmetic industry; (i) vegetable oils and fats; (j) non-saponifiable fractions of vegetable fats. Said active ingredients are used alone or in combination with one or more active ingredients from the groups (a) to (j) to produce a cosmetic and/or dermatological agent for stimulating the endogenous synthesis of barrier substances, in particular for increasing the endogenous lipid content of the skin.
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合成参考文献
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