专利号:US-2003203915-A1 优先权日:2002-04-05 标题 :Nitric oxide donors, compositions and methods of use related applications 发明人:FANG XINQIN; GARVEY DAVID S; GASTON RICKY D; LIN CHIA-EN; RANATUNGA RAMANI R; RICHARDSON STEWART K; WANG TIANSHENG; WANG WEIHENG; WEY SHIOW-JYI 权利人:FANG XINQIN; GARVEY DAVID S; GASTON RICKY D; LIN CHIA-EN; RANATUNGA RAMANI R; RICHARDSON STEWART K; WANG TIANSHENG; WANG WEIHENG; WEY SHIOW-JYI 摘要:The invention describes novel nitric oxide donors and novel compositions comprising at least one nitric oxide donor. The invention also provides novel compositions comprising at least one nitric oxide donor, and, optionally, at least one therapeutic agent. The compounds and compositions of the invention can also be bound to a matrix. The invention also provides methods for treating cardiovascular diseases, for the inhibition of platelet aggregation and platelet adhesion caused by the exposure of blood to a medical device, for treating pathological conditions resulting from abnormal cell proliferation; transplantation rejections, autoimmune, inflammatory, proliferative, hyperproliferative, vascular diseases; for reducing scar tissue or for inhibiting wound contraction, particularly the prophylactic and/or therapeutic treatment of restenosis by administering the nitric oxide donor optionally in combination with at least one therapeutic agent. The invention also provides methods for treating inflammation, pain, fever, gastrointestinal disorders, respiratory disorders and sexual dysfunctions. The nitric oxide donors donate, transfer or release nitric oxide, and/or elevate endogenous levels of endothelium-derived relaxing factor, and/or stimulate endogenous synthesis of nitric oxide and/or are substrates for nitric oxide synthase and are capable of releasing nitric oxide or indirectly delivering or transferring nitric oxide to targeted sites under physiological conditions. The therapeutic agent can optionally be substituted with at least one NO and/or NO 2 group (i.e., nitrosylated and/or nitrosated). The invention also provides novel compositions and kits comprising at least one nitric oxide donor and/or at least one therapeutic agent.
专利号:US-6593347-B2 优先权日:1998-10-30 标题 :Nitrosated and nitrosylated nonsteroidal antiinflammatory compounds, compositions and methods of use 发明人:BANDARAGE UPUL K; DONG QING; FANG XINQIN; GARVEY DAVID S; MERCER GREGORY J; RICHARDSON STEWART K; SCHROEDER JOSEPH D; WANG TIANSHENG 权利人:NITROMED INC 摘要:The present invention describes novel nitrosated and/or nitrosylated nonsteroidal antiinflammatory compounds, and novel compositions comprising at least one nitrosated and/or nitrosylated nonsteroidal antiinflammatory compound, 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. The present invention also provides methods for treating, preventing and/or reducing inflammation, pain, and fever; decreasing or reversing the gastrointestinal, renal and other toxicities resulting from the use of nonsteroidal antiinflammatory drugs; treating and/or preventing gastrointestinal disorders; treating inflammatory disease states and disorders; and treating and/or preventing ophthalmic diseases or disorders.
专利号:WO-0063184-A1 优先权日:1999-04-16 标 题:Method for producing 2-(alkylthio)-4-chloropyrimidines 发明人:RODUIT JEAN-PAUL 权利人:LONZA AG; RODUIT JEAN PAUL 摘要:The invention relates to 2- (alkylthio) -4- chloropyrimidines of general formula (I), wherein R<1> represents C1-6 alkyl and R<2> and R<3> are, independently of each other, hydrogen or C1-6 alkyl. Said chloropyrimidines are produced from the corresponding 4- hydroxy-2- mercaptopyrimidines which are reacted with a C1-6 alkyl halide to produce the corresponding 2- (alkylthio) -4- hydroxypyrimidine. The reaction product is subsequently chlorinated with phosgene. The 2- (alkylthio) -4- chlorpyrimidines are intermediate products in the synthesis of fungicides and beta-blockers.
专利号:HR-P20220848-T1 优先权日:2017-07-28 标 题:INTERMEDIATES USEFUL FOR THE SYNTHESIS OF AMINOPYRIMIDINE DERIVATIVES, PROCEDURE FOR THEIR PRODUCTION, AND PROCEDURE FOR THE PRODUCTION OF AMINOPYRIMIDINE DERIVATIVES USING THEM
专利号:US-6936600-B2 优先权日:1999-04-01 标题:Sorbitol dehrydrogenase inhibitors 发明人:CHU-MOYER MARGARET Y; MYLARI BANAVARA L; ZEMBROWSKI WILLIAM J 权利人:PFIZER 摘要:This invention is directed to sorbitol dehydrogenase inhibitory compounds of the formula I, n n nwherein R 1 , R 2 and R 3 are as defined in the specification. This invention is also directed to pharmaceutical compositions containing those compounds and methods of treating or preventing diabetic complications, particularly diabetic neuropathy, diabetic nephropathy, diabetic microangiopathy, diabetic macroangiopathy and diabetic cardiomyopathy by administering such compounds to a mammal suffering from diabetes and therefore at risk for developing such complications. This invention is also directed to pharmaceutical compositions comprising a combination of a compound of formula I of this invention with an aldose reductase inhibitor and to methods of treating or preventing diabetic complications therewith. This invention is also directed to pharmaceutical compositions comprising a combination of a compound of formula I of this invention with an NHE-1 inhibitor and to methods of treating cardiomyopathy and other heart-related problems therewith. This invention is also directed to certain intermediates used in the synthesis of the compounds of formula I and to processes for preparing those intermediates.
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