专利号:US-8901304-B1 优先权日:2013-11-05 标题:Benzo[D]imidazole derivatives of piperidine and piperazine 发明人:ULLAH NISAR 权利人:UNIV KING FAHD PET & MINERALS; KING ABDULAZIZ CITY SCI & TECH 摘要:The benzo[d]imidazole derivatives of piperidine and piperazine are 5-piperazinyl and 5-piperadinyl-1H-benzo[d]imidazol-2(3H)-ones that exhibit D 2 and 5-HT 1A receptor binding affinities, making them suitable for use as the active ingredient of pharmaceuticals for the treatment of schizophrenia. The derivatives have the general formula: n nwhere X is carbon or nitrogen and R is a selected biaryl group, or a pharmaceutically acceptable salt thereof. The piperidinyl compounds are prepared by removal of the Boc group from tert-Butyl-4-(2-oxo-2,3-dihydro-1H-benzo[d]imidazol-5-yl)piperidine-1-carboxylate. Subsequent reductive amination with a selected biarylaldehyde completes the synthesis of the 5-piperazinyl-1H-benzo[d]imidazol-2(3H)-ones. The piperazinyl compounds are prepared by preparation of the intermediate tert-Butyl 4-(3,4-diaminophenyl)piperazine-1-carboxylate. Removal of the Boc group and subsequent reductive amination with a selected biarylaldehyde completes the synthesis of the 5-piperazinyl-1H-benzo[d]imidazol-2(3H)-ones.
专利号:US-2004029774-A1 优先权日:2002-08-06 标 题:Composition and methods for the treatment of musculoskeletal disorders and collagen and elastin deficiencies 发明人:GAMAY ALY 摘要:Disclosed is a composition and method of enhanced nutrients delivery system for the treatment of musculoskeletal disorders and promotion of collagen and elastin synthesis in mammals by the oral administration of gel-like composition of hydrated Chondoritin, Glucosamine, MSM (Methyl-Sulfonyl-Methane), gelatin, hydrolyzed gelatin, collagen, and/or hydrolyzed collagen in combination with gelling agents. The increased bioavailability of the composition aids in the relief of joint pain and rebuilds cartilages, tendons, muscles, skin and connective tissues.
专利号:US-9742034-B2 优先权日:2012-12-26 标题 :Cyano-benzimidazole salts for electrochemical cells and method for synthesis thereof 发明人:CHERN YAW-TERNG; JENG JYH-LONG; CHEN SZU-YUAN; WEI AN-SHING; HWANG BING-JOE 权利人:UNIV NAT TAIWAN SCIENCE TECH 摘要:The present invention discloses a new metal cyano-substituted benzimidazolide salt having formula (I) and its preparation. This new cyano-substituted benzimidazole derivatives exhibited excellent thermal stability. The organic salt of the present invention were soluble in an alkyl carbonate solvent, such as propylene carbonate (PC), dimethyl carbonate (DMC) and ethylene carbonate (EC)/DMC cosolvent. The non-aqueous electrolyte prepared by mixing the organic metal salt of the present invention with the alkyl carbonate solvent shows high conductivity and excellent electrochemical stability. The non-aqueous electrolyte is suitable for use in primary or secondary rechargeable batteries.
专利号:US-9708336-B2 优先权日:2014-01-22 标题 :Metallo-beta-lactamase inhibitors 发明人:MANDAL MIHIR; TANG HAIFENG; XIAO LI; SU JING; LI GUOQING; YANG SHU-WEI; PAN WEIDONG; TANG HAIQUN; DEJESUS REYNALDA; HICKS JACQUELINE; LOMBARDO MATTHEW; CHU HONG; HAGMANN WILLIAM; PASTERNAK ALEX; GU XIN; JIANG JINLONG; DONG SHUZHI; DING FA-XIANG; LONDON CLARE; BISWAS DIPSHIKHA; YOUNG KATHERINE; HUNTER DAVID N; ZHAO ZHIQIANG; YANG DEXI 权利人:MERCK SHARP & DOHME 摘要:The present invention relates to compounds of formula (I) that are metallo-β-lactamase inhibitors, the synthesis of such compounds, and the use of such compounds for use with β-lactam antibiotics for overcoming resistance.
专利号:US-9745253-B2 优先权日:2015-03-13 标 题 :Alpha-cinnamide compounds and compositions as HDAC8 inhibitors 发明人:BAIR KENNETH W; Barczak Nicholas; HAN BINGSONG; LANCIA JR DAVID R; LIU CUIXIAN; MARTIN MATTHEW W; NG PUI YEE; Rudnitskaya Aleksandra; THOMASON JENNIFER R; ZABLOCKI MARY MARGARET; ZHENG XIAOZHANG 权利人:FORMA THERAPEUTICS INC 摘要:The present invention relates to inhibitors of histone deacetylases, in particular HDAC8, that are useful for the treatment of cancer and other diseases and disorders, as well as the synthesis and applications of said inhibitors.
专利号:US-8518952-B2 优先权日:2008-08-06 标题 :6 substituted 2-heterocyclylamino pyrazine compounds as CHK-1 inhibitors 发明人:BRAGANZA JOHN FREDERICK; COLLINS MICHAEL RAYMOND; KATH JOHN CHARLES; NINKOVIC SACHA; LI HUI; RICHTER DANIEL TYLER 权利人:BRAGANZA JOHN FREDERICK; COLLINS MICHAEL RAYMOND; KATH JOHN CHARLES; NINKOVIC SACHA; LI HUI; RICHTER DANIEL TYLER; PFIZER 摘要:The present invention is directed to compounds of formula (I), n nand pharmaceutically acceptable salts thereof, their synthesis, and their use as CHK-1 inhibitors.