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在 溶剂黄146体系中,用 水 作为反应溶剂,化学反应 1.0H,反应生成 丙硫氧嘧啶
参考文献: 4-Phenyl-Pyrimidine-2-Carbonitrile Derivatives[fr] Derives 4-Phenyle-Pyrimidine-2-Carbonitrile
标题: 4-Phenyl-Pyrimidine-2-Carbonitrile Derivatives[fr] Derives 4-Phenyle-Pyrimidine-2-Carbonitrile
摘要:该发明涉及具有通式(i)或其药学上可接受的盐的4-苯基嘧啶-2-羰基衍生物.该发明还涉及包含上述衍生物的药物组合物,以及在制备适用于治疗骨质疏松症,动脉粥样硬化,炎症和免疫性疾病(如类风湿性关节炎)以及神经病理性疼痛(如神经病性疼痛)的药物中的使用.

专利信息

专利号:US-8754058-B2
优先权日:2009-09-29
标 题:Inhibitors of FAM3B gene, inhibitor compositions, inhibiting methods and applications of inhibitors in preparing pharmaceuticals
发明人：GUAN YOUFEI; LIANG ZICAI
权利人:GUAN YOUFEI; LIANG ZICAI; SUZHOU RIBO LIFE SCIENCE COMPANY LTD
摘要:Inhibitors that can inhibit expression of FAM3B gene to reduce the levels of expression products, or can combine the expression products to reduce the activity of promoting lipid synthesis of FAM3B gene product are provided, wherein the inhibitors are one or more inhibitors selected from the group consisting of small interfering RNAs, antisense oligonucleotides, antibodies against FAM3B proteins and active organic compounds. Cells, vectors or inhibitor compositions, comprising such inhibitors, methods for inhibiting expression of FAM3B gene or inhibiting the activity of promoting lipid synthesis of FAM3B gene product using the inhibitors are provided. Methods for treating diseases mediated by expression of FAM3B gene using such inhibitors and uses of the inhibitors in preparing pharmaceuticals for preventing and/or treating the disease mediated by FAM3B gene expression are also provided.

专利号:EP-1382327-A1
优先权日:2002-07-17
标 题 :Method of protection of the skin against ageing
发明人：DANOUX LOUIS; FREIS OLGA; PAULY GILLES
权利人:COGNIS FRANCE SA
摘要:A method for the production of means for the stimulation of human is proposednSkin cells as well as to protect against skin aging and damaging influencesnEnvironmental toxins and UV radiation, characterized in that the means at least onenSubstance containing the synthesis of energy donors of the mitochondrial respiratory chainnincreases while at the same time the rate of reactive oxygen species (ROS) innCell metabolism lowers.n n n Furthermore, the use of cosmetic and / or pharmaceutical preparations,ncontaining at least one substance which the synthesis of energy donorsnthe mitochondrial respiratory chain increases while at the same time the rate of reactive oxygen speciesn(ROS) in cell metabolism, to stimulate human skin cellsnas well as to the protection against skin aging and damaging influences by environmental poisons andnUV radiation proposed.

专利号:US-10799441-B2
优先权日:2011-06-06
标题:Skin treatments containing pyrroloquinoline quinone (PQQ) esters and methods of preparation and use thereof
发明人：LEWIS II JOSEPH ABERNATHY; DINARDO JOSEPH C
权利人:LEWIS II JOSEPH ABERNATHY; DINARDO JOSEPH C; PCR TECH HOLDINGS LC
摘要:The present invention relates to cosmetic or dermatological compositions containing PQQ or its esters, methods of treating or promoting skin changes by topical application of these compositions, and methods of synthesis of PQQ esters. The PQQ ester-containing compositions of the present invention are unexpectedly effective in treating skin, particularly with respect to skin tolerance. When included in a topical composition, the PQQ esters of the present invention have an antioxidant effect that is useful in treating a skin change.

专利号:US-2005080260-A1
优先权日:2003-04-22
标 题 :Preparation of prodrugs for selective drug delivery
发明人：MILLS RANDELL L; WU GUO-ZHANG
摘要:Synthesis of a chemical compound having the formula A-B-C that may serve for applications such as drug delivery where A is a chemiluminescent, moiety, B is a photochromic moiety, and C is a biologically active moiety where A-B-C may serve as a prodrug. Novel synthetic methods of the present invention to form the prodrug comprised the steps of (1) forming a benzophenone, (2) forming a diaryl ethylene, (3) attaching a phthalimide moiety to at least one of the aryl groups of the ethylene to form a phthalimide-ethylene conjugate, (4) condensing two ethylene-phthalimide conjugates to form a phthalimide-pentadiene conjugate, (5) converting the phthalimide to the phthalhydrazide by reaction with hydrazine to form a carrier compound according to the present invention, and (6) reacting the carrier compound with an nucleophilic moiety of the drug to form the corresponding prodrug. Alternatively the carrier can be prepared by using the halo-substituted diaryl ethylene to make the corresponding cationic leuco dye-like compound with known methods. The cationic compound then is protected by reacting with a nucleophile and coupled with the aminophathalimide by palladium-catalyzed amination to form the protected phthalimide-pentadiene conjugate. The latter is refluxed with hydrazine to convert its phthalimide to the phthalhydrazide and acidified to give the carrier. An additional aspect of the present invention relates to the use of these compounds as antiviral agents for the treatment of viral infections such as HIV and as anticancer agents for the treatment of cancers such as bowel, lung, and breast cancer.

专利号:US-8378072-B2
优先权日:2006-04-13
标题 :Methods for designing and synthesizing directed sequence polymer compositions via the directed expansion of epitope permeability
发明人：BONNIN DUSTAN
权利人:DECLION PHARMACEUTICALS INC; BONNIN DUSTAN
摘要:The instant invention comprises a process for the solid phase synthesis of directed epitope peptide mixtures useful in the modulation of unwanted immune responses, 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.

专利号:US-11773060-B2
优先权日:2016-05-25
标题 :Method for synthesis of 9-cis-beta-carotene and formulations thereof
发明人：GAZIT EHUD; BUZHANSKY LUDMILA; IOFFE MICHAEL; SAYER ALON
权利人:UNIV RAMOT
摘要:A formulation includes an active agent, a thickening/solidifying agent, and an antioxidant. The active agent is 9-cis-β-carotene (9CBC) or a derivative thereof of the following formula:where R2 is H or methyl; X isoptionally substituted with one or more methyl groups; n is an integer of 0-16; and the asterisk represents the point of attachment to the cyclohexene ring.