专利号:US-8378099-B2 优先权日:1994-10-28 标 题:Boronic ester and acid compounds, synthesis and uses 发明人:ADAMS JULIAN; MA YU-TING; STEIN ROSS L; BAEVSKY MATTHEW; GRENIER LOUIS; PLAMONDON LOUIS 权利人:MILLENNIUM PHARMACUETICALS INC; ADAMS JULIAN; STEIN ROSS L; BAEVSKY MATTHEW; GRENIER LOUIS; PLAMONDON LOUIS 摘要:Disclosed herein is a method for reducing the rate of degradation of proteins in an animal, comprising contacting cells of the animal with certain boronic ester and acid compounds. Also disclosed herein are novel boronic ester and acid compounds, their synthesis and uses.
专利号:US-6967107-B2 优先权日:2004-02-12 标 题 :N-aryl-carbamic acid ester-derived and valeric acid ester-derived cross-linkers and conjugates, and methods for their synthesis and use 发明人:BUECHLER KENNETH F; BANASZCZYK MARIUSZ G; NOAR JOSEPH BARRY 权利人:BIOSITE INC 摘要:The present invention describes carbamic acid ester-derived and valeric acid ester-derived polyfunctional cross-linker molecules, and methods for their synthesis and use. The inclusion of polymeric moieties such as poly(alkylene oxide) in the cross-linkers of the present invention can provide advantageous solubility properties in aqueous environments. Such cross-linkers may be used to form conjugates for use in a variety of assay formats.
专利号:US-7612106-B2 优先权日:2004-12-23 标题 :Fused pyrazole derivatives and methods of treatment of metabolic-related disorders thereof 发明人:BOATMAN P DOUGLAS; SCHRADER THOMAS O; SEMPLE GRAEME; SKINNER PHILIP J; JUNG JAE-KYU 权利人:ARENA PHARM INC 摘要:The present invention relates to certain fused pyrazole derivatives of Formula (Ia), and pharmaceutically acceptable salts thereof, which exhibit useful pharmacological properties, for example, as agonists for the RUP25 receptor. n nAlso provided by the present invention are pharmaceutical compositions containing compounds of the invention, and methods of using the compounds and compositions of the invention in the treatment of metabolic-related disorders, including dyslipidemia, atherosclerosis, coronary heart disease, insulin resistance, type 2 diabetes, Syndrome-X and the like. In addition, the present invention also provides for the use of the compounds of the invention in combination with other active agents such as those belonging to the class of α-glucosidase inhibitors, aldose reductase inhibitors, biguanides, HMG-CoA reductase inhibitors, squalene synthesis inhibitors, fibrates, LDL catabolism enhancers, angiotensin converting enzyme (ACE) inhibitors, insulin secretion enhancers, DP receptor antagonists, and the like.
专利号:US-10906888-B2 优先权日:2016-07-14 标 题:Pyrimidine carboxamides as inhibitors of Vanin-1 enzyme 发明人:CASIMIRO-GARCIA AGUSTIN; STROHBACH JOSEPH WALTER; HEPWORTH DAVID; LOVERING FRANK ELDRIDGE; CHOI CHULHO; ALLAIS CHRISTOPHE PHILIPPE; WRIGHT STEPHEN WAYNE 权利人:PFIZER 摘要:Compounds, pharmaceutically acceptable salts thereof, are disclosed wherein the compounds have the structure of (I) as defined in the specification. Corresponding pharmaceutical compositions, methods of treatment, methods of synthesis, and intermediates are also disclosed.
专利号:US-10253004-B2 优先权日:2017-01-26 标 题:Indanylaminopyrazinylcyclopropanecarboxylic acids, pharmaceutical compositions and uses thereof 发明人:ECKHARDT MATTHIAS; WAGNER HOLGER; PETERS STEFAN 权利人:BOEHRINGER INGELHEIM INT 摘要:The present invention relates to compounds of formula I, n nwherein the groups R, R 1 , R 2 , R 3 , m and n are defined herein, which have valuable pharmacological properties, in particular bind to the GPR40 receptor and modulate its activity. The compounds are suitable for treatment and prevention of diseases which can be influenced by this receptor, such as metabolic diseases, in particular diabetes type 2. Furthermore, the invention relates to novel intermediates, useful for the synthesis of compounds of formula I.
专利号:US-4656291-A 优先权日:1985-03-15 标 题 :Process for producing amidine sulfonic acids 发明人:MARYANOFF CYNTHIA A; PLAMPIN JAMES N; STANZIONE ROBIN C 权利人:MCNEILAB INC 摘要:An efficient synthesis of quanidines, e.g. of the formula (III), by oxidizing a thiourea, e.g. of the following formula (II): with H2O2 and a molybdenum catalyst to yield an aminoiminomethane sulfonic acid which can then be reacted with an amine followed by optional transamination steps.