专利号:US-8354536-B2 优先权日:2008-10-13 标 题 :Diazonium-free method to make an indazole intermediate in the synthesis of bicyclic 5-(trifluormethoxy)-1H-3-indazolecarboxylic acid amides 发明人:CLEARY THOMAS; JI YAOHUI; RAWALPALLY THIMMA 权利人:HOFFMANN LA ROCHE; CLEARY THOMAS; JI YAOHUI; RAWALPALLY THIMMA 摘要:The present invention provides novel methods for preparing 5-(trifluoromethoxy)-1H-3-indazolecarboxylic acid (3), which is a useful precursor for the preparation of bicyclic-5-trifluoromethoxy-1H-indazole-3-carboxylic acid amides of Formula (1). Compounds of Formula (1) are active as agonists and partial agonists of the nicotinic α-7 receptor and are being studied for their use in the treatment of disease conditions associated with defective or malfunctioning nicotinic acetylcholine receptors, especially of the brain, such as for the treatment of Alzheimer's disease and schizophrenia, as well as other psychiatric and neurological disorders. The present methods are useful for preparing compound (3) on scale up levels.
专利号:US-2011263540-A1 优先权日:2008-07-25 标题 :Small-molecule inhibitors of protein synthesis inactivating toxins 发明人:PANG YUAN-PING; TUMER NILGUN EREKEN; MILLARD CHARLES B 权利人:PANG YUAN-PING; TUMER NILGUN EREKEN; MILLARD CHARLES B 摘要:Small-molecule inhibitors of a protein synthesis inhibiting toxin, e.g., ricin, abrin, Shiga, and Shiga-like toxins, as well as methods of using the inhibitors are provided. Further provided are methods of identifying small-molecule inhibitors of a protein synthesis inhibiting toxin.
专利号:WO-0053313-A2 优先权日:1999-03-09 标 题:Lanthanide catalysts for synthesis of compounds and combinatorial libraries
专利号:US-8497296-B2 优先权日:2011-03-31 标 题:N,N′-hydrazino-bis-isatin derivatives with selective activity against multidrug-resistant cancer cells 发明人:HASSAN TAREK ABOUL-FADL MOHAMED; KADI ADNAN AHMED; ABDEL-AZIZ HATEM ABDEL-KHADER 权利人:HASSAN TAREK ABOUL-FADL MOHAMED; KADI ADNAN AHMED; ABDEL-AZIZ HATEM ABDEL-KHADER; UNIV KING SAUD 摘要:The invention is directed to a compound of Formula (I), n nwherein R is selected from the group consisting of hydrogen atom and unsubstituted or substituted phenyl group; R 1 is selected from the group consisting of hydrogen atom and unsubstituted or substituted phenyl group; X is selected from the group consisting of hydrogen atom or halogen atom; and Y is selected from the group consisting of hydrogen atom, halogen atom, C 1 -C 4 alkyl group, nitro group, and —OCF 3 group, as well as for its use in therapy, preferably for the treatment of cancer, and to a related pharmaceutical composition, the use of the compound for the manufacture of a medicament for the respective medical indication, and a method of synthesis of the compounds of the invention.
专利号:US-2012259120-A1 优先权日:2008-10-13 标题 :Diazonium-free method to make an indazole intermediate in the synthesis of bicyclic 5-(trifluormethoxy)-1h-3-indazolecarboxylic acid amides
专利号:US-8933248-B2 优先权日:2012-06-21 标 题:3-substituted-3-hydroxy oxindole derivatives and process for preparation thereof 发明人:RAO MANDAPATI MOHAN; PRATHIMA PARVATHANENI SAI 权利人:COUNCIL SCIENT IND RES 摘要:The present invention relates to expedient method for synthesis of 3-substituted-3-hydroxy-oxindole derivatives, which are useful as synthetic precursors to valuable pharmaceutical compounds. These are synthesized by reacting nitromethane with the corresponding isatins of formula (I). The reaction process of isatins was carried using water as a solvent at room temperature to form the corresponding 3-hydroxy-3-nitromethylindolin-2-ones of formula (II).