CAS: 1572-10-7; 3-Amino-5-Phenylpyrazole

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苯甲酰乙腈置于一水合肼体系中,用 乙醇 用作溶剂,化学反应生成3-氨基-5-苯基吡唑
参考文献:设计,合成和评估2-芳基-7-(3',4'-二烷氧基苯基)-吡唑并[1,5-A ]嘧啶作为新型pde-4抑制剂
标题:设计,合成和评估2-芳基-7-(3',4'-二烷氧基苯基)-吡唑并[1,5-A ]嘧啶作为新型pde-4抑制剂
摘要:本文描述了新颖的2-芳基-7-(3',4'-二烷氧基苯基)-吡唑并[1,5-A ]嘧啶系列的新颖系列的设计,合成和生物学评估,该抑制剂可作为4型磷酸二酯酶(pde4)的抑制剂被认为是治疗哮喘和copd的好靶标.为此目的,使用已知的x射线晶体学,借助于基于结构的药物设计进行结构优化.此外,通过使用体外测定法评估了这些化合物对目标酶的生物学作用,从而产生了有效且选择性的pde-4抑制剂(ic 50 <10 Nm).
Doi:10.1016/j.Bmcl.2009.12.070

专利信息

专利号:US-5714127-A
优先权日:1992-10-08
标题 :System for multiple simultaneous synthesis
发明人：DEWITT SHEILA H H; KIELY JOHN S; PAVIA MICHAEL R; SCHROEDER MEL C; STANKOVIC CHARLES J
权利人:WARNER LAMBERT CO
摘要:A system for the multiple, simultaneous synthesis of compounds preferably uses a reaction apparatus comprising a reservoir rack having a plurality of reaction 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 has ports to allow introduction/maintenance of a controlled environment. The manifold top wall has a plurality of apertures in axial alignment with the reaction tubes and a gasket which allows penetration by a needle in order to dispense and aspirate materials from the reaction tubes. Sealing members, such as gaskets, are placed between the holder block, manifold and reservoir rack and the components are releasably fastened together. A robotic sample processor is used to automate the synthesis process using the reaction apparatus.

专利号:US-5702672-A
优先权日:1992-10-08
标 题 :Apparatus and method for multiple simultaneous synthesis
发明人：DEWITT SHEILA H H; KELL MICHAEL; PAVIA MICHAEL R; KIELY JOHN S; SCHROEDER MEL C; STANKOVIC CHARLES J; WARE STEVEN
权利人:WARNER LAMBERT CO
摘要:An apparatus for multiple, simultaneous synthesis of compounds which 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.

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:US-5567391-A
优先权日:1992-10-08
标题 :Apparatus for multiple simultaneous synthesis
发明人：DEWITT SHEILA H H; KIELY JOHN S; PAVIA MICHAEL R; SCHROEDER MEL C; STANKOVIC CHARLES J
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-9630393-A1
优先权日:1995-03-27
标 题:A method for the synthesis of mixtures of compounds
发明人：BECKER KATHERINE; DEWITT SHEILA HOBBS
权利人:WARNER LAMBERT CO
摘要:Described is a method of synthesizing a plurality of compounds in a plurality of wells comprising the steps of: (a) providing a plurality of test wells in a plurality of arrays of the wells; (b) reacting in at least a one step reaction a first reagent with a plurality of reagents called building blocks in the test well to obtain a unique product designed to be the same in each array; and (c) continuing to react reagents such that there are multiple reagents resulting in mixtures of multiple different products in each well.

专利号:US-10995078-B2
优先权日:2013-03-13
标 题:Compounds and compositions for inhibition of FASN
发明人：BAIR KENNETH W; LANCIA JR DAVID R; LI HONGBIN; LOCH JAMES; LU WEI; MARTIN MATTHEW W; MILLAN DAVID S; SCHILLER SHAWN E R; TEBBE MARK J
权利人:FORMA THERAPEUTICS INC
摘要:The present invention relates to compounds and composition for inhibition of FASN, their synthesis, applications, and antidotes. An illustrative compound of the invention is shown below: