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1. 发明申请

WO2007127683A3 ADMINISTRATION OF AGONIST-ANTAGONIST IN OPIOID-DEPENDENT PATIENTS 审中-公开
标题翻译：阿片类依赖患者中的AGONIST-ANTAGONIST的治疗
公开(公告)号：WO2007127683A3
公开(公告)日：2008-10-30
申请号：PCT/US2007067101
申请日：2007-04-20
申请人： VORONKOV MICHAEL VICTOR , NEZHINSKY EFIM DAVID , ISAKULYAN LEVON GEVORKOVICH , OCHERET DARIA ALEXANDROVNA
发明人： VORONKOV MICHAEL VICTOR , NEZHINSKY EFIM DAVID , ISAKULYAN LEVON GEVORKOVICH , OCHERET DARIA ALEXANDROVNA
IPC分类号： A61K38/05
CPC分类号： A61K9/2027 , A61K9/2054 , A61K31/485
摘要： A method for reducing psychological opioid dependence includes selecting a patient addicted to an opioid and administering to the patient an opioid agonist-antagonist for at least 14 days, thereby reducing craving for the opioid in the patient. An opioid agonist-antagonist is administered in a patient needing an average adherence to a treatment protocol of at least 95 percent. A non-injectable formulation containing an agonist-antagonist also is disclosed.
摘要翻译：减少心理阿片样物质依赖的方法包括选择上瘾的阿片样物质的患者，并向患者施用阿片样物质激动剂 - 拮抗剂至少14天，从而减少对患者中阿片样物质的渴望。在需要至少95％的治疗方案的平均依从性的患者中施用阿片样物质激动剂 - 拮抗剂。还公开了含有激动剂 - 拮抗剂的不可注射制剂。

2. 发明申请

WO2007016674A3 2-AMINOARYL PYRIDINES AS PROTEIN KINASES INHIBITORS 审中-公开
标题翻译： 2-氨基吡啶作为蛋白激酶抑制剂
公开(公告)号：WO2007016674A3
公开(公告)日：2007-03-15
申请号：PCT/US2006030269
申请日：2006-07-31
申请人： LEXICON GENETICS INC , AUGERI DAVID , TARVER JAMES , FU QINGHONG , VORONKOV MICHAEL VICTOR , HACKLEY DOAN , MERTZMAN MICHAEL E , CARLSEN MARIANNE
发明人： AUGERI DAVID , TARVER JAMES , FU QINGHONG , VORONKOV MICHAEL VICTOR , HACKLEY DOAN , MERTZMAN MICHAEL E , CARLSEN MARIANNE
IPC分类号： C07D401/10 , A61K31/4418 , A61K31/4436 , A61K31/4439 , A61K31/501 , C07D213/50 , C07D401/04 , C07D401/14 , C07D417/10
CPC分类号： C07D401/04 , C07D213/73 , C07D401/10 , C07D417/10
摘要： Aryl pyridines of formula (I), compositions comprising them, and their use for the protein kinases related disorders are described.
摘要翻译：描述式（I）的芳基吡啶，包含它们的组合物及其用于蛋白激酶相关病症的用途。

3. 发明申请

WO2007127683A2 ADMINISTRATION OF AGONIST-ANTAGONIST IN OPIOID-DEPENDENT PATIENTS 审中-公开
标题翻译：阿片类依赖患者中的AGONIST-ANTAGONIST的行政管理
公开(公告)号：WO2007127683A2
公开(公告)日：2007-11-08
申请号：PCT/US2007/067101
申请日：2007-04-20
申请人： VORONKOV, Michael Victor , NEZHINSKY, Efim David , ISAKULYAN, Levon Gevorkovich , OCHERET, Daria Alexandrovna
发明人： VORONKOV, Michael Victor , NEZHINSKY, Efim David , ISAKULYAN, Levon Gevorkovich , OCHERET, Daria Alexandrovna
IPC分类号： A61K9/14
CPC分类号： A61K9/2027 , A61K9/2054 , A61K31/485
摘要： A method for reducing psychological opioid dependence includes selecting a patient addicted to an opioid and administering to the patient an opioid agonist-antagonist for at least 14 days, thereby reducing craving for the opioid in the patient. An opioid agonist-antagonist is administered in a patient needing an average adherence to a treatment protocol of at least 95 percent. A non-injectable formulation containing an agonist-antagonist also is disclosed.
摘要翻译：减少心理阿片样物质依赖的方法包括选择上瘾的阿片样物质的患者，并向患者施用阿片样物质激动剂 - 拮抗剂至少14天，从而减少对患者中阿片样物质的渴望。在需要至少95％的治疗方案的平均依从性的患者中施用阿片样物质激动剂 - 拮抗剂。还公开了含有激动剂 - 拮抗剂的不可注射制剂。

4. 发明申请

WO2006091450A1 4-PIPERIDIN-1-YL-7H-PYRROLO[2,3-D]PYRIMIDINE COMPOUNDS 审中-公开
标题翻译： 4-PIPERIDIN-1-YL-7H-吡咯[2,3-D]吡啶化合物
公开(公告)号：WO2006091450A1
公开(公告)日：2006-08-31
申请号：PCT/US2006/005335
申请日：2006-02-15
申请人： LEXICON GENETICS INCORPORATED , RAWLINS, David Brent , VORONKOV, Michael Victor , ZHANG, Yulian
发明人： RAWLINS, David Brent , VORONKOV, Michael Victor , ZHANG, Yulian
IPC分类号： C07D487/04 , A61K31/519 , A61P35/00
CPC分类号： C07D487/04
摘要： Substituted 4-piperidin-l -yl-7H-pyrrolo[2,3-D]pyrirnidine compounds are disclosed, as well as compositions comprising them and methods of their use for the treatment, prevention and management of various diseases and disorders.
摘要翻译：公开了取代的4-哌啶-1-基-7H-吡咯并[2,3-D]嘧啶化合物，以及包含它们的组合物及其用于治疗，预防和治疗各种疾病和病症的方法。

5. 发明申请

WO2007016674A2 ARYL PYRIDINES AND METHODS OF THEIR USE 审中-公开
标题翻译： ARYL PYRIDINES及其使用方法
公开(公告)号：WO2007016674A2
公开(公告)日：2007-02-08
申请号：PCT/US2006/030269
申请日：2006-07-31
申请人： LEXICON GENETICS INCORPORATED , AUGERI, David , TARVER, James , FU, Qinghong , VORONKOV, Michael Victor , HACKLEY, Doan , MERTZMAN, Michael E. , CARLSEN, Marianne
发明人： AUGERI, David , TARVER, James , FU, Qinghong , VORONKOV, Michael Victor , HACKLEY, Doan , MERTZMAN, Michael E. , CARLSEN, Marianne
IPC分类号： C07D401/10 , C07D417/10 , C07D401/04 , A61K31/4439
CPC分类号： C07D401/04 , C07D213/73 , C07D401/10 , C07D417/10
摘要： Aryl pyridines, compositions comprising them, and methods of their use for the treatment, prevention and management of a variety of diseases and disorders are disclosed.
摘要翻译：公开了芳基吡啶，包含它们的组合物及其用于治疗，预防和治疗各种疾病和病症的方法。

6. 发明申请

WO0246149A3 2-THIO-5-AMINO SUBSTITUTED BENZOQUINONES, THEIR MANUFACTURE AND THEIR USE IN RUBBER 审中-公开
标题翻译： 2-THIO-5-AMINO取代苯并噻唑，其制造及其在橡胶中的用途
公开(公告)号：WO0246149A3
公开(公告)日：2003-03-13
申请号：PCT/US0146374
申请日：2001-12-05
申请人： FLEXSYS AMERICA LP , MAENDER OTTO W , ROSTEK CHARLES JOHN , KATRITZKY ALAN ROY , ODENS HERMAN HOWARD , VORONKOV MICHAEL VICTOR
发明人： MAENDER OTTO W , ROSTEK CHARLES JOHN , KATRITZKY ALAN ROY , ODENS HERMAN HOWARD , VORONKOV MICHAEL VICTOR
IPC分类号： C07C323/30 , C07C323/45 , C07C323/52 , C07D209/08 , C07D295/112 , C08K5/372 , C07D213/70 , C07D239/38 , C07D295/10
CPC分类号： C07D295/112 , C07C323/30 , C07C323/45 , C07C323/52 , C07C2601/14 , C07C2601/16 , C07D209/08 , C08K5/3725 , C08L21/00
摘要： The invention comprises a process for preparing a compound having the formula where Z and W are the same or different, and selected from the group consisting of O, NH and NR, where R is H, alkyl, cycloalkyl or aryl, R' is alkyl, cycloalkyl, alkylene, alkyl 3-propionate, aryl or arylene. A is H if either or both of Z and W are not O, but if both Z and W are O, A is (I) or a carbon based heterocyclic component having an amine constituent, or RR''N-, where R'' is the same or different than R and is selected from the same group as R. The process comprises preparing an alkylthio-substituted benzoquinone intermediate by reacting in a first reaction mixture a thiosubstituted aromatic having the formula (II) where X is OH, NH2 or NHR when Z is O, NH or NR, respectively, and where Y is OH, NH2 or NHR when W is O, NH or NR, respectively, with an alkali metal periodate in the presence of a phase transfer catalyst, followed, if A is not H, by reacting the intermediate in a second reaction mixture containing an amine included in the group of amines comprising A, and in the presence of oxygen to obtain the compound. If A is H no second reaction mixture is employed and the intermediate comprises the compound. The invention includes a process for making the composition and the use of the composition in natural and synthetic rubber, and with monomers, gasoline and lubricating oil to inhibit polymerization.
摘要翻译：本发明包括一种制备具有下式的化合物的方法，其中Z和W相同或不同，并且选自O，NH和NR，其中R是H，烷基，环烷基或芳基，R'是烷基，环烷基，亚烷基，3-丙酸烷基酯，芳基或亚芳基。如果Z和W都不是O，则A是H，但如果Z和W都是O，则A是（I）或具有胺组分的碳基杂环组分或RR“N - ，其中R' '与R相同或不同，并且选自与R相同的基团。该方法包括通过在第一反应混合物中使具有式（II）的取代的芳族化合物（其中X为OH，NH 2 当Z为O，NH或NR时，分别为NH，NH或NHR，当相转移催化剂存在时，当W为O，NH或NR时，其中Y为OH，NH2或NHR， A不是H，通过使中间体在包含包含A组胺的胺的第二反应混合物中和在氧气存在下反应以获得化合物。如果A为H，则不使用第二反应混合物，中间体包含该化合物。本发明包括在天然和合成橡胶中制备组合物和使用组合物以及单体，汽油和润滑油以抑制聚合的方法。

7. 发明申请

WO2009021169A3 (7H-PYRR0L0 [2, 3-D] PYRIMIDIN-4-YL) -PIPERAZINES AS KINASE INHIBITORS FOR THE TREATMENT OF CANCER AND INFLAMMATION 审中-公开
标题翻译：（7H-PYRR0L0 [2,3-D]嘧啶-4-YL） - 作为激素治疗和感染的激酶抑制剂
公开(公告)号：WO2009021169A3
公开(公告)日：2009-04-30
申请号：PCT/US2008072584
申请日：2008-08-08
申请人： LEXICON PHARMACEUTICALS INC , HARRISON BRYCE ALDEN , KIMBALL SPENCER DAVID , MABON ROSS , RAWLINS DAVID BRENT , RICE DENNIS S , VORONKOV MICHAEL VICTOR , ZHANG YULIAN
发明人： HARRISON BRYCE ALDEN , KIMBALL SPENCER DAVID , MABON ROSS , RAWLINS DAVID BRENT , RICE DENNIS S , VORONKOV MICHAEL VICTOR , ZHANG YULIAN
IPC分类号： C07D487/04 , A61K31/519 , A61P35/00
CPC分类号： C07D487/04 , C07D519/00
摘要： Inhibitors of LIM kinase 2 are disclosed, along with pharmaceutical compositions com psin them and methods of their use. X is O or NRA; Y is O, NRR, or C(RR)2; A is cycloalkyl, aryl or hctcrocyclc; RA is hydrogen, cyano, nitro, RA1, SO2RA1, SO2NRA1, or SO2N(RA1)2;
摘要翻译：公开了LIM激酶2的抑制剂，以及它们的药物组合物及其使用方法。 X是O或NRA; Y是O，NRR或C（RR）2; A是环烷基，芳基或杂环基; RA为氢，氰基，硝基，RA1，SO2RA1，SO2NRA1或SO2N（RA1）2;

8. 发明申请

WO2009021169A2 KINASE INHIBITORS, COMPOSITIONS COMPRISING THEM, AND METHODS OF THEIR USE 审中-公开
标题翻译：激素抑制剂，包含它们的组合物及其使用方法
公开(公告)号：WO2009021169A2
公开(公告)日：2009-02-12
申请号：PCT/US2008/072584
申请日：2008-08-08
申请人： LEXICON PHARMACEUTICALS, INC. , HARRISON, Bryce Alden , KIMBALL, Spencer David , MABON, Ross , RAWLINS, David Brent , RICE, Dennis S. , VORONKOV, Michael Victor , ZHANG, Yulian
发明人： HARRISON, Bryce Alden , KIMBALL, Spencer David , MABON, Ross , RAWLINS, David Brent , RICE, Dennis S. , VORONKOV, Michael Victor , ZHANG, Yulian
IPC分类号： C07D487/04 , A61K31/519 , A61P35/00
CPC分类号： C07D487/04 , C07D519/00
摘要： Inhibitors of LIM kinase 2 are disclosed, along with pharmaceutical compositions comprising them and methods of their use.
摘要翻译：公开了LIM激酶2的抑制剂，以及包含它们的药物组合物及其使用方法。

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