专利号:US-5766556-A 优先权日:1992-10-08 标题:Apparatus and method for multiple simultaneous synthesis 发明人:DEWITT SHEILA HELEN HOBBS; KIELY JOHN STEVEN; PAVIA MICHAEL RAYMOND; SCHROEDER MEL CONRAD; STANKOVIC CHARLES JOHN 权利人:WARNER LAMBERT CO 摘要:An apparatus and method which provides a suitable location for multiple, simultaneous synthesis of compounds. The apparatus consists of: a reservoir block having a plurality of wells; a plurality of reaction tubes, usually gas dispersion tubes, having filters on their lower ends; a holder block, having a plurality of apertures; and a manifold, which may have ports to allow introduction/maintenance of a controlled environment. The manifold top wall has apertures and a detachable plate with identical apertures. The apparatus is constructed from materials which will accommodate heating, cooling, agitation, or corrosive reagents. Gaskets are placed between the components. Rods or clamps are provided for fastening the components together. Apparatus operation involves placing the filters on the lower ends of the reaction tubes in the reservoir block wells, and the upper ends passing through the holder block apertures and into the manifold. The apparatus provides in excess of 1 mg of each product with structural knowledge and control over each compound. The apparatus can be adapted to manual, semiautomatic or fully automatic performance. Using the apparatus a series of building blocks are covalently attached to a solid support. These building blocks are then modified by covalently adding additional different building blocks or chemically modifying some existing functionality until the penultimate structure is achieved. This is then cleaved from the solid support by another chemical reaction into the solution within the well yielding an array of newly synthesized individual compounds, which after postreaction modification, if necessary, are suitable for testing for activity.
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:US-4171439-A 优先权日:1975-04-11 标 题 :Antibacterial analogs of isocephalosporins 发明人:CONWAY TERRY T; LIM GARY M F; MENARD MARCEL 权利人:BRISTOL MYERS CO 摘要:There is described the stereoselective total synthesis of novel DELTA 2,3-1,4-morpholine-2-carboxylic acids possessing a fused beta -lactam ring in the 1,6-position and carrying a substituent cis to carbon 5 in the 7-position of the fused ring system represented by the general formula I wherein Z is halo or hydroxyl and X is acylamino. Also included in the invention are compounds of the above formula in which the carboxyl group at the 2-position is protected as by an easily cleavable ester group and salts of both the free acids and carboxyl-protected compounds. The compounds are potent antibacterial agents.
专利号:US-4761413-A 优先权日:1986-12-22 标 题:1,5-epoxy-2,3,4,5-tetrahydro-1H-3-benzazepins and use in treatment of ulcers 发明人:WACHTER MICHAEL P; KARANEWSKY DONALD S 权利人:ORTHO PHARMA CORP 摘要:The synthesis of epoxybenzazepin compounds is described. The novel compounds have anti-ulcer activity.
专利号:US-4855426-A 优先权日:1986-12-22 标题:Process of preparing 1,5-epoxy-2,3,4,5-tetrahydro-1H-3-benzazepins 发明人:WACHTER MICHAEL P; KARANEWSKY DONALD S 权利人:ORTHO PHARMA CORP 摘要:The synthesis of epoxybenzazepin compounds is described. The novel compounds have anti-ulcer activity.
专利号:US-12364961-B2 优先权日:2021-01-13 标 题 :Multiplex synthesis method of compound library and parallel synthesizer of compound library using same 发明人:KIM DONG PYO; AHN GWANG NOH 权利人:POSTECH RES & BUSINESS DEV FOUND 摘要:The present invention relates to a parallel synthesis method and synthesizer of a compound library, and more specifically provides a parallel synthesis method and synthesizer of a compound library, which uniformly distribute a first reactant and perform independent reactions in separate spaces, and since it is possible to confirm the results for various reaction variables at once, the synthesis time of the compound library can be reduced with a high synthesis yield of the product.