专利号:US-11866398-B2 优先权日:2018-05-15 标 题:Total synthesis of prostaglandin J natural products by stereoretentive metathesis 发明人:LI JIAMING; CHEN XU; AHMED TONIA S; STOLTZ BRIAN M; GRUBBS ROBERT H 权利人:CALIFORNIA INST OF TECHN 摘要:This invention relates generally to the synthesis of Δ12-Prostaglandin J product using stereoretentive ruthenium olefin metathesis catalysts supported by dithiolate ligands. Δ12-Prostaglandin J products were generated with excellent selectivity (>99% Z) and in moderate to high/good yields (47% to 80% yield; 58% to 80% yield).
专利号:US-7772278-B2 优先权日:1999-03-01 标 题:Nitrosated and nitrosylated prostaglandins, compositions and methods of use 发明人:GARVEY DAVID S; GASTON RICKY D; LETTS L GORDON; DE TEJADA INIGO SAENZ; TAM SANG WILLIAM; WORCEL MANUEL 权利人:NITROMED INC 摘要:The invention describes novel nitrosated and/or nitrosylated prostaglandins, and novel compositions comprising at least one nitrosated and/or nitrosylated prostaglandin, and, optionally, at least one compound that donates, transfers or releases nitric oxide, elevates endogenous levels of endothelium-derived relaxing factor, stimulates endogenous synthesis of nitric oxide or is a substrate for nitric oxide synthase, and/or at least one vasoactive agent. The invention also provides novel compositions comprising at least one prostaglandin and at least one S-nitrosothiol compound, and, optionally, at least one vasoactive agent. The prostaglandin is preferably a prostaglandin E 1 compound, more preferably alprostadil, and the S-nitrosothiol compound is preferably S-nitrosoglutathione. The invention also provides methods for treating or preventing sexual dysfunctions in males and females, for enhancing sexual responses in males and females, and for treating or preventing cerebrovascular disorders, cardiovascular disorders, benign prostatic hyperplasia (BPH), glaucoma, peptic ulcers or for inducing abortions.
专利号:WO-2024020091-A1 优先权日:2022-07-19 标 题 :Inhibitors of short-chain dehydrogenase activity for reducing glial fibrillary acidic protein levels 发明人:MARKOWITZ SANFORD; PIEPER ANDREW 权利人:UNIV CASE WESTERN RESERVE; THE US GOV AS REPRESENTED BY THE DEPARTMENT OF VETERAN AFFAIRS 摘要:A method of decreasing blood glial fibrillary acidic protein (GFAP) levels in a subject in need thereof includes administering to the subject a therapeutically effective amount of a 15-PGDH inhibitor. Astroglia cells are the major and perhaps most abundant cell types in the brain. In healthy brain, astrocytes help with providing structural and network support for neurons and interface with the brain vasculature, including the blood-brain-barrier. Functionally, astrocytes are involved with providing neurotrophic factors (such as glial derived neurotrophic factor (GDNF)), and cytokine/chemokine release that influences the global and local inflammatory response environments, as well as working closely with neurons involved in the glutamate-glutamine synthesis/recycling pathway.
专利号:WO-0054773-A1 优先权日:1999-03-12 标题:Dopamine agonists in combination with nitric oxide donors, compositions and methods of use 发明人:GARVEY DAVID S 权利人:NITROMED INC; GARVEY DAVID S 摘要:The present invention is directed to novel compositions comprising at least one dopamine agonist in combination with at least one nitric oxide donor (i.e. compounds that donate, transfer or release nitric oxide, elevate endogenous levels of endothelium-derived relaxing factor, stimulate endogenous synthesis of nitric oxide or are substrates for nitric oxide synthase). The novel compositions may optionally comprise at least one therapeutic agent, such as, a vasoactive agent, an antimetic agent, and mixtures thereof. The dopamine agonist is preferably apomorphine. The present invention is also directed to methods for treating and/or preventing sexual dysfunctions and/or enhancing sexual responses in patients. In other embodiments, the present invention is directed to methods treating or preventing neurodegenerative diseases, mitochondrial diseases, spinal cord injury, central or psychostimulant addiction, senile dementia, circulatory disorders, cardiovascular disorders, hyperprolactinaemia or myopia. The compounds and/or compositions of the present invention can also be provided in the form of a pharmaceutical kit.
专利号:US-11407837-B2 优先权日:2017-09-11 标 题 :GPCR binding proteins and synthesis thereof 发明人:GLANVILLE JACOB 权利人:TWIST BIOSCIENCE CORP 摘要:Provided herein are methods and compositions relating to G protein-coupled receptor (GPCR) libraries having nucleic acids encoding for a scaffold comprising a GPCR binding domain. Libraries described herein include variegated libraries comprising nucleic acids each encoding for a predetermined variant of at least one predetermined reference nucleic acid sequence. Further described herein are protein libraries generated when the nucleic acid libraries are translated. Further described herein are cell libraries expressing variegated nucleic acid libraries described herein.
专利号:CN-116947724-A 优先权日:2022-04-14 标 题:Synthesis method of latanoprost
1: Pursley JR, Martins JP, Wright C, Stewart ND. Compared to dinoprost tromethamine, cloprostenol sodium increased rates of estrus detection, conception and pregnancy in lactating dairy cows on a large commercial dairy. Theriogenology. 2012 Sep 1;78(4):823-9. doi: 10.1016/j.theriogenology.2012.03.032. Epub 2012 May 22. Epub 2006 Nov 28.
合成参考文献
参考文献:10.1016/0739-7240(96)00069-0 摘要:Wade DE, Lewis GS. Exogenous prostaglandin F2 alpha stimulates utero-ovarian release of prostaglandin F2 alpha in sheep: a possible component of the luteolytic mechanism of action of exogenous prostaglandin F2 alpha. Domest Anim Endocrinol. 1996 Sep;13(5):383–98. doi: 10.1016/0739-7240(96)00069-0. 参考文献:10.1016/s0378-4320(99)00026-3 摘要:Manik RS, Singla SK, Palta P, Madan ML. Changes in follicular populations following treatment of buffaloes with PMSG (eCG) and Neutra-PMSG for superovulation. Anim Reprod Sci. 1999 May 17;56(1):31–8. doi: 10.1016/s0378-4320(99)00026-3. 参考文献:10.3168/jds.2010-3650 摘要:Martins JP, Policelli RK, Pursley JR. Luteolytic effects of cloprostenol sodium in lactating dairy cows treated with G6G/Ovsynch. J Dairy Sci. 2011 Jun;94(6):2806–14. doi: 10.3168/jds.2010-3650. 参考文献:10.3168/jds.2010-3652 摘要:Martins JP, Policelli RK, Neuder LM, Raphael W, Pursley JR. Effects of cloprostenol sodium at final prostaglandin F2α of Ovsynch on complete luteolysis and pregnancy per artificial insemination in lactating dairy cows. J Dairy Sci. 2011 Jun;94(6):2815–24. doi: 10.3168/jds.2010-3652. 参考文献:10.1111/j.1439-0396.2008.00830.x 摘要:Roy KS, Prakash BS. Plasma progesterone, oestradiol-17β and total oestrogen profiles in relation to oestrous behaviour during induced ovulation in Murrah buffalo heifers. J Anim Physiol Anim Nutr (Berl). 2009 Aug;93(4):486–95. doi: 10.1111/j.1439-0396.2008.00830.x.