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131. 发明公开

EP0618843A1 PHOSPHONIC ACID BASED ION EXCHANGE RESINS 失效
标题翻译：基于膦酸的离子交换树脂
公开(公告)号：EP0618843A1
公开(公告)日：1994-10-12
申请号：EP93901924.0
申请日：1992-12-18
申请人： ARCH DEVELOPMENT CORPORATION , THE UNIVERSITY OF TENNESSEE RESEARCH CORPORATION
发明人： HORWITZ, E., Philip , ALEXANDRATOS, Spiro, D. , GATRONE, Ralph, C. , CHIARIZIA, Ronato
IPC分类号： B01D15 , B01J39
CPC分类号： B01J39/20 , B01J39/12
摘要： Résines échangeuses d'ions permettant d'extraire les ions métalliques d'un flux de liquides usés. Une résine échangeuse d'ions est préparée en copolymérisant un acide disphosphonique vinylidène avec du styrène, de l'acrylnitryle et du divinyl benzène.
摘要翻译：离子交换树脂，用于从废液中提取金属离子。离子交换树脂通过亚乙烯基二膦酸与苯乙烯，丙烯酰基和二乙烯基苯的共聚来制备。

132. 发明公开

EP0380588A4 CERTAIN 3-SUBSTITUTED 2-ALKYL BENZOFURAN DERIVATIVES 失效转让
标题翻译：某些3-取代的2-烷基苯并呋喃衍生物
公开(公告)号：EP0380588A4
公开(公告)日：1991-04-03
申请号：EP88910246
申请日：1988-09-28
申请人： THE UNIVERSITY OF TENNESSEE RESEARCH CORPORATION
发明人： KENNEDY, THOMAS, P. , KABALKA, GEORGE, W.
IPC分类号： C07D307/81 , A61K31/34 , A61K31/343 , A61P9/00 , A61P9/08 , C07D307/80 , C07D307/18 , C07D405/10 , C07D407/10
CPC分类号： C07D307/80
摘要： The disclosure relates to compounds of formula (I) and pharmaceutically acceptable addition salts thereof wherein X represents a single, direct bond or a substituted or unsubstituted alkylene chain containing 1 to 4 carbon atoms, wherein R5 is a lower alkyl group, wherein R6 is either hydrogen or methyl, wherein Am is selected from the class consisting of amino, lower mono and dialkylamino, piperidino, piperazino, N-lower alkyl piperazino, pyrrrolidino, and morpholino groups wherein Y1 and Y2 are identical and are hydrogen, a halogen, methyl or ethyl and n is an integer in the range of 1-5. They are useful in treating arrhythmic conditions and conditions for which treatment with a vasodilator is indicated.

133. 发明公开

EP0380588A1 CERTAIN 3-SUBSTITUTED 2-ALKYL BENZOFURAN DERIVATIVES 失效转让
标题翻译：某些取代的3-烷基-2-苯并呋喃衍生物。
公开(公告)号：EP0380588A1
公开(公告)日：1990-08-08
申请号：EP88910246.0
申请日：1988-09-28
申请人： THE UNIVERSITY OF TENNESSEE RESEARCH CORPORATION
发明人： KENNEDY, Thomas, P. , KABALKA, George, W.
IPC分类号： C07D307 , A61K31 , A61P9
CPC分类号： C07D307/80
摘要： L'invention concerne des composés de la formule (I) et ses sels d'addition pharmaceutiquement acceptables, dans laquelle X représente une liaison directe unique ou une chaîne d'alkylène à substitution ou sans substitution contenant 1 à 4 atomes de carbone, R5 représente un groupe alkyle inférieur, R6 représente soit de l'hydrogène soit du méthyle, Am est choisi dans une classe composée de groupes amino, mono et dialkylamino inférieurs, de piperidino, de piperazino, de pyrrolidino, et de morpholino, Y1 et Y2 sont identiques et représentent de l'hydrogène, un halogène, du méthyle ou de l'éthyle, et n est un nombre entier compris entre 1 et 5.

134. 发明公开

EP0300682A1 A homogeneous, lipsome-based signal amplification method for assays involving enzymes 失效
标题翻译： Ein匀浆，au f。。。。。。。。。。。。。。。。。。。。。。。。。。。。。。
公开(公告)号：EP0300682A1
公开(公告)日：1989-01-25
申请号：EP88306427.1
申请日：1988-07-13
申请人： THE UNIVERSITY OF TENNESSEE RESEARCH CORPORATION
发明人： Huang, Leaf
IPC分类号： G01N33/58 , C12Q1/68 , G01N33/74 , G01N33/53
CPC分类号： G01N33/581 , A61K9/1271 , G01N33/586
摘要： The present invention is directed to a procedure for enhancing the enzyme-dependent readout of diagnostic assays using specially prepared liposomes.
Microgenic's CEDIA assay for digoxin was employed as an illustrative example of the present invention. The magnitude of signal was only 25 mA/min/ng digoxin/ml for the unamplified assay, while the signal magnitude for the amplified (i.e., liposome-enhanced) assay was 1,000 mA/min/ng digoxin/mL, i.e., a 40-fold amplification.
Stable liposomes were prepared with unsaturated PE stabilized with 5 mole percent of ganglioside GM₁. Glucose-6-phosphate dehydrogenase (G6PHD) was entrapped in these unilamellar liposomes in high concentrations. Addition of beta-galactosidase (B-gal) caused rapid (3-5 min.) lysis of liposomes revealing the latent G6PDH activity, due to the enzymatic degalactosylation of MG₁.
This simple, rapid and homogenous signal amplification procedure will be useful in many enzyme dependent assays, such as ELISA, CEDIA, Gene-probe assays and Immunoliposome assays.
摘要翻译：本发明涉及使用特别制备的脂质体来增强诊断测定酶的酶依赖性读出的方法。作为本发明的说明性实施例，使用了用于地高辛的微生物CEDIA测定。对于未扩增测定，信号的幅度仅为25mA / min / ng地高辛/ ml，而扩增（即，脂质体增强）测定的信号幅度为1,000mA / min / ng地高辛/ mL，即40 倍放大。用5摩尔％的神经节苷脂GM1稳定的不饱和PE制备稳定的脂质体。葡萄糖-6-磷酸脱氢酶（G6PHD）以高浓度包埋在这些单层脂质体中。加入β-半乳糖苷酶（B-gal）引起脂质体的快速（3-5分钟）裂解，显示由于MG1的酶脱羧基化而引起潜在的G6PDH活性。这种简单，快速和均匀的信号扩增程序将在许多酶依赖性测定中有用，例如ELISA，CEDIA，基因探针测定和免疫脂质体测定。

135. 发明公开

EP1918287A3 LPA receptor agonists and antagonists and methods of use 审中-公开
标题翻译： LPA受体激动剂和拮抗剂和使用方法
公开(公告)号：EP1918287A3
公开(公告)日：2008-08-20
申请号：EP07122187.3
申请日：2001-03-19
申请人： THE UNIVERSITY OF TENNESSEE RESEARCH CORPORATION
发明人： Miller, Duane , Tigyi, Gabor , Dalton, James , Sardar, Vineet , Elrod, Don , Xu, Huiping , Baker, Daniel , Wang, Dean , Liliom, Karoly , Fischer, David , Virag, Tamas , Nusser, Nora
IPC分类号： C07D327/00 , C07D327/06 , C07F9/06 , C07F9/38 , C07F9/10 , A61K31/66
CPC分类号： C07F9/4028 , A61K31/27 , A61K31/66 , C07F9/091 , C07F9/093 , C07F9/094 , C07F9/098 , C07F9/11 , C07F9/17 , C07F9/222 , C07F9/3808
摘要： The present invention relates to compounds according to formula (I) as disclosed herein as well as pharmaceutical compositions which include those compounds Also disclosed are methods of using such compounds, which have activity as agonists or as antagonists of LPA receptors: such methods including inhibiting LPA activity on an LPA receptor, modulating LPA receptor activity, treating cancer, enhancing cell proliferation, and treating a wound.

136. 发明公开

EP1633733A1 CANNABINOID DERIVATIVES, METHODS OF MAKING, AND USE THEREOF 有权
标题翻译：大麻素衍生物，用于生产及其用途
公开(公告)号：EP1633733A1
公开(公告)日：2006-03-15
申请号：EP04752828.6
申请日：2004-05-20
申请人： THE UNIVERSITY OF TENNESSEE RESEARCH CORPORATION
发明人： MOORE, Bob, M., II , FERREIRA, Antonio, M. , KRISHNAMURTHY, Mathangi
IPC分类号： C07D311/80 , C07D405/06 , C07D405/14 , C07D407/06 , A61K31/35
CPC分类号： C07D409/04 , C07D311/80
摘要： 1'-substituted cannabinoid derivatives of delta-8-tetrahydrocannabinol, delta-9-tetrahydrocannabinol, and delta-6a-10a-tetrahydrocannabinol that have affinity for the cannabinoid receptor type-1 (CB-1) and/or cannabinoid receptor type2 (CB-2). Compounds having activity as either agonists or antagonists of the CB-1 and/or CB-2 receptors can be used for treating CB-1 or CB-2 mediated conditions.

137. 发明授权

EP1023284B1 ANTI-VIRAL PHARMACEUTICAL COMPOSITIONS CONTAINING SATURATED 1,2-DITHIAHETEROCYCLIC COMPOUNDS 失效
标题翻译：饱和1,2- DITHIAHETEROCYCLISCHE含抗病毒药物制剂
公开(公告)号：EP1023284B1
公开(公告)日：2005-11-23
申请号：EP97942372.0
申请日：1997-07-03
申请人： THE GOVERNMENT OF THE UNITED STATES OF AMERICA, as represented by THE SECRETARY, DEPARTMENT OF HEALTH AND HUMAN SERVICES , THE UNIVERSITY OF TENNESSEE RESEARCH CORPORATION
发明人： RICE, William, G. , SCHULTZ, Robert, R. , BAKER, David, C. , HENDERSON, Louis, E.
IPC分类号： C07D339/04 , C07D339/08 , A61K31/385 , A61P31/12 , A61P31/14 , A61P31/16 , A61P31/18 , A61P31/20 , A61P31/22 , A61P43/00
CPC分类号： C07D339/04 , A61K31/385 , A61K45/06 , C07D339/08
摘要： The present invention is directed to pharmaceutical compositions including a saturated 1,2-dithiaheterocyclic compound having anti-viral activity. The present invention also provides a kit containing the pharmaceutical composition and methods of treating or preventing viral disease using the composition, as well as methods for inactivating retrovirus in a body fluid.

138. 发明公开

EP1491524A3 Selective androgen receptor modulators and methods of use thereof 有权
标题翻译：雄激素受体的选择性调节剂及其使用方法
公开(公告)号：EP1491524A3
公开(公告)日：2005-04-20
申请号：EP04019299.9
申请日：2001-08-23
申请人： THE UNIVERSITY OF TENNESSEE RESEARCH CORPORATION
发明人： Dalton, James , Miller, Duane, D. , Yin, Donghua , He, Yali
IPC分类号： C07C233/15 , C07C233/33 , C07C233/48 , C07C235/26 , C07C237/14 , A01N37/18 , A01N31/16 , C07C235/24 , A61K31/167
CPC分类号： C07D215/227 , A61K31/167 , A61K31/404 , A61K31/4706 , A61K31/661 , C07C235/24 , C07D209/08 , C07D271/12 , G01N33/5438 , G01N33/74
摘要： This invention provides a novel class of androgen receptor targeting agents (ARTA). The agents define a new subclass of compounds which are tissue-selective androgen receptor modulators (SARM), which are useful for oral testosterone replacement therapy, male contraception, maintaining sexual desire in women, treating prostate cancer and imaging prostate cancer. These agents have an unexpected in-vivo activity for an androgenic and anabolic activity of a nonsteroidal ligand for the androgen receptor. These agents may be active alone or in combination with progestins or estrogens. The invention further provides a novel class of nonsteroidal agonist compounds and methods of binding an androgen receptor, modulating spermatogenesis, treating and imaging prostate cancer, and providing hormonal therapy for androgen-dependent conditions.

139. 发明公开

EP1491524A2 Selective androgen receptor modulators and methods of use thereof 有权
标题翻译：雄激素受体激动剂和方法
公开(公告)号：EP1491524A2
公开(公告)日：2004-12-29
申请号：EP04019299.9
申请日：2001-08-23
申请人： THE UNIVERSITY OF TENNESSEE RESEARCH CORPORATION
发明人： The designation of the inventor has not yet been filed
IPC分类号： C07C233/15 , C07C233/33 , C07C233/48 , C07C235/26 , C07C237/14 , A01N37/18 , A01N31/16 , C07C235/24 , A61K31/167
CPC分类号： C07D215/227 , A61K31/167 , A61K31/404 , A61K31/4706 , A61K31/661 , C07C235/24 , C07D209/08 , C07D271/12 , G01N33/5438 , G01N33/74
摘要： This invention provides a novel class of androgen receptor targeting agents (ARTA). The agents define a new subclass of compounds which are tissue-selective androgen receptor modulators (SARM), which are useful for oral testosterone replacement therapy, male contraception, maintaining sexual desire in women, treating prostate cancer and imaging prostate cancer. These agents have an unexpected in-vivo activity for an androgenic and anabolic activity of a nonsteroidal ligand for the androgen receptor. These agents may be active alone or in combination with progestins or estrogens. The invention further provides a novel class of nonsteroidal agonist compounds and methods of binding an androgen receptor, modulating spermatogenesis, treating and imaging prostate cancer, and providing hormonal therapy for androgen-dependent conditions.
摘要翻译：选择性雄激素受体调节剂丙酰胺衍生物（I）是新的。式（I）的选择性雄激素受体调节剂丙酰胺衍生物是新的。 X：O，CH 2，NH，Se，PR或NR; Z：NO 2，CN，COR，COOH或CONHR; Y：I，CF 3，Br，Cl或SnR 3; Q：烷基，H，NR 2，NHCOCH 3，NHCOCF 3，NHCOR，NHCONHR，NHCCOR，OCONHR，CONHR，NHCSCH 3，NHCSCF 3，NHCSR，NHSO 2CH 3，NHSO 2，OR，COR，OCOR，OSO 2，SO 2R或SR; 或Q：式（i） - （iii）的稠合环; R：烷基，芳基，1-4C（卤代）烷基，苯基，卤素，烯基或OH; R 1：CH 3，CF 3，CH 2 CH 3或CF 2CF 3; 和T：OH，OR，NHCOCH 3或NHCOR。包括以下独立权利要求：（1）调节精子发生的方法，包括施用（I）; （2）一种激素治疗方法，其包括给予（I）; （3）治疗激素相关病症的方法，包括施用（I）; 和（4）治疗前列腺癌的方法，其包括施用（I）。活动：细胞抑制。作用机制：雄激素受体调节剂。确定选择性雄激素受体调节剂化合物（I）的体外活性。 N- [4-硝基-3-三氟甲基） - 苯基] - （2S）-3- [4-（乙酰氨基） - 苯氧基] -2-羟基-2-甲基丙酰胺（Ia）与雄激素受体结合为7.5nM。

140. 发明公开

EP1427424A2 LPA RECEPTOR AGONISTS AND ANTAGONISTS AND METHODS OF USE 审中-公开
标题翻译： LPA受体激动剂和拮抗剂及其使用方法
公开(公告)号：EP1427424A2
公开(公告)日：2004-06-16
申请号：EP02773455.7
申请日：2002-09-17
申请人： THE UNIVERSITY OF TENNESSEE RESEARCH CORPORATION
发明人： MILLER, Duane, D. , TIGYI, Gabor , DALTON, James, T. , SARDAR, Vineet, M. , ELROD, Don, B. , XU, Huiping , BAKER, Daniel, L. , WANG, Dean , LILIOM, Karoly , FISCHER, David, J. , VIRAG, Tamas , NUSSER, Nora
IPC分类号： A61K31/66 , A61K31/07 , A61K47/00
CPC分类号： C07F9/11 , A61K31/27 , A61K31/66 , A61K31/663 , C07C237/06 , C07C237/08 , C07C271/22 , C07F9/091 , C07F9/093 , C07F9/094 , C07F9/098 , C07F9/17 , C07F9/222 , C07F9/3808 , C07F9/4028
摘要： The present invention relates to compounds according to formula (I) as disclosed herein as well as pharmaceutical compositions which include those compounds. Also disclosed are methods of using such compounds, which have activity as agonists or as antagonists of LPA receptors; such methods including inhibiting LPA activity on an LPA receptor, modulating LPA receptor activity, treating cancer, enhancing cell proliferation, treating a wound, treating apoptosis or preserving or restoring function in a cell, tissue, or organ, culturing cells, preserving organ or tissue function, and treating a dermatological condition.

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