专利号:US-8835680-B1 优先权日:2011-05-13 标题 :Stereospecific synthesis process for tretinoin compounds 发明人:DENG QINGJUN; WANG SHAOHUI; ZHU QIANG; GAO TAIPING; LI YONGSHENG 权利人:DENG QINGJUN; WANG SHAOHUI; ZHU QIANG; GAO TAIPING; LI YONGSHENG; CHONGQING HUABANGSHENGKAI PHARM CO LTD 摘要:A stereospecific synthesis process for tretinoin compounds comprises the following steps: using substituted triphenyl phosphine salt and β-formyl crotonic acid as raw material to carry out WITTIG reaction under the action of alkali; then adjusting the pH of the reaction liquid to 5-10; adding palladium compound or rhodium compound to carry out isomerization directly and obtain tretinoin compounds with desired configuration. The product yield of the process is high and the intermediate product in the reaction dose not need to be separated. The process is easy to operate and can save the production cost and as well is suitable for industrial production.
专利号:US-6787668-B2 优先权日:2000-04-13 标 题 :2-amino-4,5 heptenoic acid derivatives useful as nitric oxide synthase inhibitors 发明人:PITZELE BARNETT S; SIKORSKI JAMES A; WEBBER RONALD KEITH 权利人:PHARMACIA CORP 摘要:The present invention is directed to a compound of formula I:or a pharmaceutically acceptable salt thereof, wherein:R1 is selected from the group consisting of H and methyl; andR2 is selected from the group consisting of H and methyl.The compounds possess useful nitric oxide synthetase inhibiting activity, and are expected to be useful in the treatment or prophylaxis of a disease or condition in which the synthesis or over synthesis of nitric oxide forms a contributory part.
专利号:US-5587396-A 优先权日:1994-08-26 标 题 :Method of ameliorating cellulite by disrupting the barrier function of the stratum corneum 发明人:SMITH WALTER P 权利人:MARY KAY INC 摘要:New topically applied treatments for cellulite are shown by comparative data to effect structural improvements in cellulite-afflicted thigh area tissues including skin-thickening, thigh-firming and thigh-reduction. The disclosed treatments disrupt the skin's water barrier and elevate trans-epidermal water loss (TEWL) for extended periods of weeks or months and include methods of mechanical or solvent action, for example, tape stripping, or acetone washes. Preferred treatments use creams with active ingredients such as lactic acid to elevate TEWL, a retinoid, preferably vitamin A palmitate to disrupt barrier rebuilding and prolong elevation of TEWL levels, and a cerebroside to inhibit lipid synthesis and intensify the TEWL elevation. Diuretics, for immediate esthetic improvements, anti-irritants and anti-oxidants for irritation control are optional ingredients.
专利号:WO-2006040676-A1 优先权日:2004-10-12 标题 :Nitrosated benzopyran compounds as novel cyclooxygenase-2 selective inhibitors 发明人:TJOENG FOE SIONG; CARTER JEFFERY; SPRINGER JOHN ROBERT; ZUPEC MARK E 权利人:PHARMACIA & UPJOHN CO LLC; TJOENG FOE SIONG; CARTER JEFFERY; SPRINGER JOHN ROBERT; ZUPEC MARK E 摘要:This invention specifically relates to novel cyclooxygenase 2 (COX-2) selective inhibitor compounds that donate, transfer or release nitric oxide, stimulate endogenous synthesis of nitric oxide, elevate endogenous levels of endothelium-derived relaxing factor or is a substrate for nitric oxide synthase. Compounds of particular interest and their analogs defined by formula (I) wherein Z, X, R1, R2, R3, and R4 are as described in the specification. This invention also relates to pharmaceutical compositions and methods for treating COX-2 mediated disorders, such as inflammation and inflammation related disorders.
专利号:US-6316465-B1 优先权日:1998-06-27 标 题:Ophthalmic uses of PPARgamma agonists and PPARgamma antagonists 发明人:PERSHADSINGH HARRIHAR A; LEVY DANIEL E 权利人:PHOTOGENESIS INC 摘要:Methods of treating diseases of ocular tissues expressing the nuclear receptor PPARgamma, by inhibiting the inflammatory response, the neovascularization and angiogenesis, and programmed cell death (apoptosis) in these target tissues, comprising administering to a human or animal in need of treatment an effective amount of a compound that modifies the activity of PPARgamma, or pharmaceutically acceptable salts and solvates thereof.Novel compounds and methods for their synthesis are provided, including a compound having the general structure:
专利号:US-7772246-B2 优先权日:2007-08-01 标题:Pyrazole compounds as RAF inhibitors 发明人:CUI JINGRONG JEAN; DEAL JUDITH GAIL; GU DANLIN; GUO CHUANGXING; JOHNSON MARY CATHERINE; KANIA ROBERT STEVEN; KEPHART SUSAN ELIZABETH; LINTON MARIA ANGELICA; MCALPINE INDRAWAN JAMES; PAIRISH MASON ALAN; PALMER CYNTHIA LOUISE 权利人:PFIZER 摘要:The present invention is directed to compounds of Formula (I), n nand to pharmaceutically acceptable salts thereof, their synthesis, and their use as Raf inhibitors.
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