序号 | 专利名 | 申请号 | 申请日 | 公开(公告)号 | 公开(公告)日 | 发明人 |
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141 | AZULENYL NITRONE SPIN TRAPPING AGENTS, METHODS OF MAKING AND USING SAME | PCT/US2005034091 | 2005-09-22 | WO2006036768A3 | 2006-09-28 | BECKER DAVID; LEY JAMES JOSEPH |
The present invention provides azulenyl nitrones, such as those having the following general formula: (I) compositions comprising the same and methods of their use for the treatment or prevention of oxidative, ischemic, ischemia/reperfusion-related and chemokine-mediated conditions. | ||||||
142 | DECREASE IN OXIDATIVE STRESS STATUS THROUGH THE ADMINISTRATION OF NATURAL PRODUCTS AND PHARMACEUTICAL DRUGS | PCT/US2005019018 | 2005-05-20 | WO2005112915A3 | 2006-03-16 | CUTLER RICHARD G |
The present invention provides compositions, methods, and kits for reducing oxidative stress thereby extending life span. The compositions, methods, and kits of the present invention can also be used to treat diseases of aging resulting from oxidative stress. | ||||||
143 | CETP INHIBITORS | PCT/US2005/012196 | 2005-04-08 | WO2005100298A1 | 2005-10-27 | ALI, Amjad; BOHN, Joann; DENG, Qiaolin; LU, Zhijian; SINCLAIR, Peter, J.; TAYLOR, Gayle, E.; THOMPSON, Christopher, F.; QURAISHI, Nazia |
Compounds of Formula (I), including pharmaceutically acceptable salts of the compounds, are CETP inhibitors, and are useful for raising HDL-cholesterol, reducing LDL-cholesterol, and for treating or preventing atherosclerosis. In the compounds of Formula 1, A1 and A2 are each an aromatic ring, a 5-6-membered heterocyclic ring, an aromatic ring fused to a heterocyclic ring, a phenyl ring fused to a heterocyclic ring, or a cycloalkyl ring. |
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144 | COMPOUNDS FOR THE TREATMENT OF METABOLIC DISORDERS | PCT/US2004012142 | 2004-04-20 | WO2004093806A3 | 2005-04-07 | HODGE KIRVIN L; KAUFMAN ROBERT J; LEE ALBERT; SHARMA SHALINI; VON BORSTEL REID W |
Agents useful for the treatment of various metabolic disorders, such as insulin resistance syndrome, diabetes, hyperlipidemia, fatty liver disease, cachexia, obesity, atherosclerosis and arteriosclerosis are disclosed. Formula (I) wherein n is 1 or 2; m is 2 or 3; q is 0 or 1; t is 0 or 1; R<2> is alkyl having from 1 to 3 carbon atoms; R<3> is hydrogen, halo, alkyl having from 1 to 3 carbon atoms, or alkoxy having from 1 to 3 carbon atoms; A is phenyl, unsubstituted or substituted by 1 or 2 groups selected from: halo, alkyl having 1 or 2 carbon atoms, perfluoromethyl, alkoxy having 1 or 2 carbon atoms, and perfluoromethoxy; or cycloalkyl having from 3 to 6 ring carbon atoms wherein the cycloalkyl is unsubstituted or one or two ring carbons are independently mono-substituted by methyl or ethyl; or a 5 or 6 membered heteroaromatic ring having 1 or 2 ring heteroatoms selected from N, S and O and the heteroaromatic ring is covalently bound to the remainder of the compound of formula I by a ring carbon; and R<1> is hydrogen or alkyl having 1 or 2 carbon atoms. Alternatively, when R<1> is hydrogen, the biologically active agent can be a pharmaceutically acceptable salt of the compound of Formula (I). | ||||||
145 | LIPOPHILIC DIESTERS OF CHELATING AGENT FOR INHIBITION OF ENZYME ACTIVITY | PCT/IL0300225 | 2003-03-16 | WO2004028443A3 | 2004-05-27 | STRIEM SARINA; FRIEDMAN JONATHAN EDUARD; REZNITSKY-COHEN DALIA; KOZAK ALEXANDER |
The present invention relates to the use of lipophilic diesters of the chelating agent 1,2-bis(2 aminophenoxy)ethane-N,N,N',N'-tetraacetic acid (BAPTA) for inhibition of proteolytic activities of certain metalloproteinases and of calpain. The invention further relates to methods for preventing, treating or managing MMP-related and calpain-related diseases or disorders in mammals comprising administering to a mammal in need thereof, a pharmaceutical composition comprising a therapeutically effective amount of said lipophilic diesters of the chelating agent BAPTA. | ||||||
146 | PREPARATION OF POLYARYL CARBOXYLIC ACIDS | PCT/US0205606 | 2002-02-26 | WO02076382A3 | 2003-04-03 | QIAN ZHENRONG; SU HENG ERIC; DEWITT LEE ALAN |
Disclosed are methods for preparing polyaromatic carboxylic acids or salts thereof by reacting an aromatic boronic acid with a haol-substituted aromatic carboxylic acid or salt thereof. | ||||||
147 | PROPANOIC ACID DERIVATIVES THAT INHIBIT THE BINDING OF INTEGRINS TO THEIR RECEPTORS | PCT/US0012464 | 2000-05-05 | WO0068188A9 | 2002-08-29 | BIEDIGER RONALD J; HOLLAND GEORGE W; KASSIR JAMAL M; LI WEN; MARKET ROBERT V; SCOTT IAN L; WU CHENGDE |
A method for the inhibition of the binding of alpha 4 beta 1 integrin to its receptors, for example VCAM-1 (vascular cell adhesion molecule-1) and fibronectin; compounds that inhibit this binding; pharmaceutically active compositions comprising such compounds; and the use of such compounds either as above, or in formulations for the control or prevention of diseases states in which alpha 4 beta 1 is involved. | ||||||
148 | CASPASE INHIBITORS AND THE USE THEREOF | PCT/US2000/009319 | 2000-04-07 | WO00061542A1 | 2000-10-19 | |
The present invention is directed to novel dipeptide thereof, represented by general formula (I): where R1-R3, X and Y are defined herein. The present invention also relates to the discovery that compounds having Formula (I) are potent inhibitors of caspases and apoptotic cell death. Therefore, the inhibitors of this invention can retard or block cell death in a variety of clinical conditions in which the loss of cells, tissues or entire organs occurs. | ||||||
149 | IMPROVED GAMMA AMINO BUTYRIC ACID ANALOGS | PCT/US1999/025569 | 1999-11-02 | WO00031020A1 | 2000-06-02 | |
The instant invention is improved gamma amino butyric acid analogs, processes for their preparation, and methods of using them as agents for treating epilepsy and other neurodegenerative disorders, depression, anxiety, panic, pain, neuropathological disorders, gastrointestinal damage, and inflammation. | ||||||
150 | TWO-PHOTON OR HIGHER-ORDER ABSORBING OPTICAL MATERIALS | PCT/US1999/008383 | 1999-04-16 | WO99053242A1 | 1999-10-21 | |
Disclosed are highly efficient multiphoton absorbing compounds and methods of their use. The compounds generally include a bridge of pi-conjugated bonds connecting electron donating groups or electron accepting groups. The bridge may be substituted with a variety of substituents as well. Solubility, lipophilicity, absorption maxima and other characteristics of the compounds may be tailored by changing the electron donating groups or electron accepting groups, the substituents attached to or the length of the pi-conjugated bridge. Numerous photophysical and photochemical methods are enabled by converting these compounds to electronically excited states upon simultaneous absorption of at least two photons of radiation. The compounds have large two-photon or higher-order absorptivities such that upon absorption, one or more Lewis acidic species, Lewis basic species, radical species or ionic species are formed. | ||||||
151 | alpha -AMIDES OF L-AMINO ACIDS AS FRAGRANCE PRECURSORS | PCT/US1998/025907 | 1998-12-07 | WO99030680A1 | 1999-06-24 | |
Disclosed are alpha -amides of L-amino acids that produce fragrance or attenuate or mask malodor. In particular, glutamine and asparagine amides can be used in the invention. Such alpha -amides of L-amino acids are useful for generating pleasant fragrances or attenuating or masking malodor upon cleavage of the alpha -amides of L-amino acids by bacteria in axillae. The alpha -amides of L-amino acids can be incorporated into skin treatment compositions and personal care products, such as deodorants, body sprays and antiperspirants, and used in methods for producing fragrance or attenuating or masking malodor. | ||||||
152 | PRODUCTION OF D,L-ASPARTIC ACID | PCT/US1997009205 | 1997-05-30 | WO1997047587A1 | 1997-12-18 | DONLAR CORPORATION; MAZO, Grigory, Ya; MAZO, Jacob; VALLINO, Barney, Jr.; ROSS, Robert, J. |
The present invention is directed to a method for the production of D,L-aspartic acid. The method comprises reacting an unsatured dicarboxylic acid or anhydride such as maleic acid, fumaric acid, maleic anhydride or mixtures thereof with excess aqueous ammonia at an elevated temperature and pressure for a time sufficient to produce diammonium D,L aspartate. The diammonium D,L aspartate is then neutralized to D,L-aspartic acid; excess unreacted ammonia and various by-products may be recycled and re-used in the method, thereby minimizing waste and cost; i.e. the process is useful for a continuous production process which may be represented conveniently as a schematic block diagram wherein a pressurized reactor (10) receives a reactant admixture from feed tank (12), the reactants being fed subsequently to flash vessel (14) and then precipitator (16) where D,L-aspartic acid is produced upon neutralization, with dicarboxylic acid salts being recovered in a centrifuge (18) and dried in a drier (20). The D,L-aspartic acid may subsequently be used to make polyaspartic acid. | ||||||
153 | REDUCING TETRANITROMETHANE IN COMPOSITIONS CONTAINING NITROAROMATIC COMPOUNDS | PCT/US1997005769 | 1997-04-07 | WO1997038967A1 | 1997-10-23 | ARCO CHEMICAL TECHNOLOGY, L.P.; QUAKENBUSH, Allen, B.; PENNINGTON, B., Timothy |
A process is disclosed for removing a light organic compound from a liquid composition comprising said light organic compound in admixture with a nitroaromatic compound, said light organic compound having a partial vapor pressure in said composition that is greater than the partial vapor pressure of said nitroaromatic compound in said composition, said process comprising contacting said composition with steam or a gas to cause at least a portion of said light organic compound to pass out of said composition and into admixture with said steam or gas. | ||||||
154 | 稠合三环γ-氨基酸衍生物的制备方法及中间体 | PCT/CN2019/096522 | 2019-07-18 | WO2020029762A1 | 2020-02-13 | 范江; 陈清平; 汪成涛; 冯建川 |
一种稠合三环γ-氨基酸衍生物的制备方法及中间体,和制备该稠合三环γ-氨基酸衍生物的中间体的方法。所述稠合三环γ-氨基酸衍生物具有式(Ⅰ)所示的结构。所述制备方法原料易得、步骤简单,整个合成工艺都用结晶纯化,没有用到硅胶柱层析或其他制备色谱方法,适宜大规模工业化生产。 |
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155 | 联苯化合物的制备及应用 | PCT/CN2014/070822 | 2014-01-17 | WO2015106443A1 | 2015-07-23 | 邵玉田; 熊杰; 覃小龙; 章金龙; 蔡国平; 陈邦池 |
提供联苯化合物的制备及应用。以2-硝基芳基乙烯及取代的1,3-丁二烯为原料一步得到2-氨基联苯化合物、2-硝基联苯化合物或它们的混合物;反应得到的2-硝基联苯化合物或其与2-氨基联苯化合物的混合物可还原制备2-氨基联苯化合物。以该方法制备的2-氨基联苯化合物为原料与酰氯反应可制得具有杀菌作用的酰胺化合物。该方法避免使用金属化合物、贵金属催化剂及特殊硼试剂,以简单易得化合物原料一步得到联苯化合物,工艺步骤少,后处理简单,利于工业化。 |
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156 | SYNTHETIC ACID AND ASSOCIATED METHODS | PCT/US2011/062555 | 2011-11-30 | WO2012075091A3 | 2012-06-07 | MacDONALD, John T.; MacDONALD III, John T. |
Glycine is an organic compound that can be used in the making of a synthetic acid that obviates all the drawbacks of strong acids such as hydrochloric acid. The new compound is made by dissolving glycine in water, in a weight ratio of approximately 1:1 to 1:1.5. The solution is mixed until the glycine is essentially fully dissolved in the water. Once dissolution is complete, hydrogen chloride gas is dissolved in the solution to produce the new compound, which can be referred to as hydrogen glycine. |
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157 | PHOTOCHEMICAL METHODS AND PHOTOACTIVE COMPOUNDS FOR MODIFYING SURFACES | PCT/US2006043614 | 2006-11-09 | WO2008054398A3 | 2008-10-02 | CARROLL GREGORY T; WANG DENONG; TURRO NICHOLAS J; KOBERSTEIN JEFFREY T |
Compounds and methods for controlling the surface properties are described. Compounds of the invention can form radicals upon exposure to irradiation, which can then react with nearby molecules to alter the surface properties of various substrates. The invention can provide surfaces that are resistant to dewetting, surfaces that have immobilized molecules such as carbohydrates and polymers immobilized, and surfaces that have metals deposited on the surface. The invention can be utilized in a wide range of application, such as sensors, microreactors, microarrays, electroless deposition of metals, and the like. | ||||||
158 | 光学フィルム | PCT/JP2007/000315 | 2007-03-28 | WO2007111026A1 | 2007-10-04 | 大石和也; 村田力; 森内英輝; 桑原将臣 |
透光性基体上に1層積層した構成で、防眩機能、高コントラスト化、色再現性、ギラツキ防止をバランスよく満足することのできる光学フィルムを提供する。本発明の光学フィルムは、透光性基体上に、透光性樹脂微粒子と放射線硬化型樹脂組成物とを含有した樹脂層を積層し、ヘイズ値が40~60%、0.5mm幅の光学くしを用いた透過像鮮明度が5~35%であり、樹脂層の最表面の平均傾斜角度が0.8~3.0度の微細な凹凸形状を有することを特徴とする。 |
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159 | PROCESS OF PREPARING BROMOPICRIN | PCT/IL2006000978 | 2006-08-22 | WO2007023496A3 | 2007-07-05 | OREN JAKOB; GOLAN LEAH; FRIM RON |
Process of preparing high purity bromopicrin, and high purity bromopicrin produced therefrom. Providing a mixture of nitromethane and bromine, and preferably water, and absent of organic solvent. Adding an aqueous solution of an alkaline substance to the mixture, thereby providing a reaction mixture containing bromopicrin, the adding performed such that no excess of the alkaline substance occurs in the reaction mixture during the adding. Collecting the organic phase (containing the bromopicrin) from the reaction mixture. No need for subjecting the organic phase of the reaction mixture to distillation or extraction, for obtaining near quantitative yield of bromopicrin having purity of at least equal to or greater than 96 weight percent. Process parameters controlling selectivity of reaction forming bromopicrin are molar ratio of bromine and nitromethane in the mixture; reaction temperature while bromopicrin is formed; concentration of the alkaline substance in the aqueous solution; and reaction time. | ||||||
160 | CERAMIDES AND APOPTOSIS-SIGNALING LIGAND | PCT/US2005039272 | 2005-10-31 | WO2006050265A3 | 2007-05-10 | BIELAWSKA ALICJA; HANNUN YUSUF A; NORRIS JAMES; SZULC ZDZISLAW; DONG JIAN-YUN; BIELAWSKI JACEK; SCHWARTZ DAVID; HOLMAN DAVID; EL-ZAWAHRY AHMED; MCKILLOP JOHN |
The invention provides the compounds of formula (I): and pharmaceutically acceptable salts thereof, wherein R1, R2, R3, R4, A, X, Y, a, b and n are as defined herein. Also disclosed are methods for making the compounds of formula (I) and their use in treating or preventing diseases associated with cell overproliferation and dysfunctional sphingolipid signal transduction. The invention also encompasses the use of the compounds in combination with an apoptosis-signaling ligand, such as Fas ligand. Preferably, the Fas ligand is administered in the form of a gene therapy agent. |