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21. 发明申请

WO99062893A2 NOVEL NEUROKININ ANTAGONISTS, METHOD FOR THE PRODUCTION THEREOF AND PHARMACEUTICAL COMPOSITIONS CONTAINING SAID COMPOUNDS 审中-公开
标题翻译：新NEUROKININANTAGONISTEN，方法生产它们和药物组合物含
公开(公告)号：WO99062893A2
公开(公告)日：1999-12-09
申请号：PCT/EP1999/003531
申请日：1999-05-22
IPC分类号： C07D295/14 , A61K31/4427 , A61K31/4468 , A61K31/4545 , A61K31/495 , A61K31/496 , A61K31/5375 , A61K31/5377 , A61P43/00 , C07D211/58 , C07D233/44 , C07D233/46 , C07D233/48 , C07D233/54 , C07D239/12 , C07D295/215 , C07D401/12
CPC分类号： C07D295/215 , C07C2601/14 , C07D233/44 , C07D239/12
摘要： The invention relates to novel compounds of general formula (I) or the pharmaceutically acceptable salts thereof, wherein X = N-R or CH-R , Y = CH2 or (CH2)2, Z = O or H2; and R , R , R , R and Ar have the meaning cited in the description. The invention also relates to the production and use thereof. The novel compounds are valuable neurokinin (tachykinin) antagonists.
摘要翻译：本发明涉及通式（I）或新的化合物药学上可接受的盐，其中X = N-R <3>或CH-R <4>，Y = CH 2或（CH 2）2，Z为= O或H 2; 和R <1>，R <2>，R <3>，R <4>和Ar具有在说明书中给出的含义，并且它们的制备和用途。这些新化合物是有价值的神经激肽（速激肽）拮抗剂。

22. 发明申请

WO2016085224A3 N-HETEROCYCLIC CARBENE NITRIC OXIDE RADICAL AND APPLICATION THEREOF 审中-公开
标题翻译： N-杂环碳烯一氧化氮自由基及其应用
公开(公告)号：WO2016085224A3
公开(公告)日：2016-08-11
申请号：PCT/KR2015012624
申请日：2015-11-24
申请人： INST BASIC SCIENCE , POSTECH ACAD IND FOUND
发明人： LEE EUNSUNG , KIM KIMOON , PARK JUNBEOM , SONG HAYOUNG , KIM YOUNGSUK
IPC分类号： C07D233/44 , A61K31/4164 , A61K31/4168 , C07D233/66 , C07D233/91
CPC分类号： C07D233/88 , C07D233/12
摘要： The present invention relates to an N-heterocyclic carbene nitric oxide radical, and an application thereof, and more particularly, to an N-heterocyclic carbene nitric oxide radical for effectively delivering nitric oxide having a desirable amount within a short period of time, a method for producing an N-heterocyclic carbene nitric oxide radical, and an application thereof.
摘要翻译： N-杂环卡宾氧化氮自由基及其应用技术领域本发明涉及N-杂环卡宾氧化氮自由基及其应用，并且更具体地涉及用于在短时间内有效递送具有所需量的氧化氮的N-杂环卡宾氧化氮自由基，用于制备N-杂环卡宾氧化氮自由基及其应用。

23. 发明申请

WO2016112251A1 4,5-DIHYDROIMIDAZOLE DERIVATIVES AND THEIR USE AS HISTONE DEMETHYLASE (KDM2B) INHIBITORS 审中-公开
标题翻译： 4,5-DIHYDROIMIDAZOLE衍生物及其用作HISTONE DEMETHYLASE（KDM2B）抑制剂
公开(公告)号：WO2016112251A1
公开(公告)日：2016-07-14
申请号：PCT/US2016/012588
申请日：2016-01-08
申请人： GENENTECH, INC. , CONSTELLATION PHARMACEUTICALS, INC.
发明人： ALBRECHT, Brian, K. , COTE, Alexandre , GEHLING, Victor , HSIAO-WEI TSUI, Vickie , KIEFER, James, Richard, Jr. , LIANG, Jun , MAGNUSON, Steven , NASVESCHUK, Christopher, G. , ROMERO, F. Anthony , TAYLOR, Alexander, M.
IPC分类号： C07D403/12 , C07D233/44 , C07D401/04 , C07D235/02 , C07D401/12 , C07D409/12 , C07D413/12 , C07D417/12 , C07D487/08 , A61K31/454 , A61K31/496 , A61K31/4995 , A61P35/00
CPC分类号： C07D233/44 , C07D235/02 , C07D401/04 , C07D401/12 , C07D403/12 , C07D409/12 , C07D413/12 , C07D417/12 , C07D487/08
摘要： The present invention relates to compounds of formula (I), (formula I) wherein: X is C(=0) or S(0) 2 ; R 1 is selected from the group consisting of N-linked piperazinyl, relinked piperidine, and N-linked diazabicyclo[3.2.1]octane, wherein R 1 is optionally substituted with one or more groups; R 2 and R 3 are each independently selected from H, C 1-6 alkyl, C 2-6 alkenyl, C 2-6 alkynyl, and C 3-8 cycloalkyl, wherein any C 1-6 alkyl, C 2-6 alkenyl, C 2-6 alkynyl, and C 3-8 cycloalkyl is optionally substituted with one or more groups; or R 2 and R 3 taken together with the carbon to which they are attached form a 3-, 4-, 5-, or 6-membered carbocyclic ring that is optionally substituted with one or more groups; R 4 and R 5 are each independently selected from H, C 1-6 alkyl, C 2-6 alkenyl, C 2-6 alkynyl, and C 3-8 cycloalkyl, wherein any C 1-6 alkyl, C 2-6 alkenyl, C 2-6 alkynyl, and C 3-8 cycloalkyl is optionally substituted with one or more groups; or R 4 and R 5 taken together with the carbon to which they are attached form a 3-, 4-, 5-, or 6-membered carbocyclic ring that is optionally substituted with one or more groups; and R 6 is a 5-10 membered heteroaryl, 5-10 membered heterocycle, or a 6-10 membered aryl, which 5-10 membered heteroaryl, 5-10 membered heterocycle, and 6-10 membered aryl is optionally substituted with one or more groups; useful as inhibitors of one or more histone demethylses, such as KDM2b. The invention also provides pharmaceutically acceptable compositions comprising compounds of the present invention and methods of using said compositions in the treatment of various disorders.
摘要翻译：本发明涉及式（I），（式I）的化合物，其中：X为C（= O）或S（O）2; R1选自N-连接的哌嗪基，再连接的哌啶和N-连接的二氮杂双环[3.2.1]辛烷，其中R 1任选被一个或多个基团取代; R 2和R 3各自独立地选自H，C 1-6烷基，C 2-6烯基，C 2-6炔基和C 3-8环烷基，其中任何C 1-6烷基，C 2-6烯基，C 2-6炔基和C 3-8环烷基任选被一个或更多组; 或者R 2和R 3与它们所连接的碳一起形成任选被一个或多个基团取代的3-，4-，5-或6-元碳环; R 4和R 5各自独立地选自H，C 1-6烷基，C 2-6烯基，C 2-6炔基和C 3-8环烷基，其中任何C 1-6烷基，C 2-6烯基，C 2-6炔基和C 3-8环烷基任选被一个或更多组; 或R 4和R 5与它们所连接的碳一起形成任选被一个或多个基团取代的3-，4-，5-或6-元碳环; 并且R 6是5-10元杂芳基，5-10元杂环或6-10元芳基，其中5-10元杂芳基，5-10元杂环和6-10元芳基任选被一个或多个组; 可用作一种或多种组蛋白去甲基酶的抑制剂，例如KDM2b。本发明还提供包含本发明化合物的药学上可接受的组合物和使用所述组合物治疗各种疾病的方法。

24. 发明申请

WO2013036869A2 COMPOSITIONS, METHODS, AND SYSTEMS FOR THE SYNTHESIS AND USE OF IMAGING AGENTS 审中-公开
标题翻译：用于合成和成像剂使用的组合物，方法和系统
公开(公告)号：WO2013036869A2
公开(公告)日：2013-03-14
申请号：PCT/US2012/054309
申请日：2012-09-07
申请人： LANTHEUS MEDICAL IMAGING, INC. , RADEKE, Heike, S. , CESATI, Richard, R. , PUROHIT, Ajay , HARRIS, Thomas, D. , ROBINSON, Simon, P. , YU, Ming , CASEBIER, David, S. , HU, Carol, Hui , BROEKEMA, Matthias , ONTHANK, David, C.
发明人： RADEKE, Heike, S. , CESATI, Richard, R. , PUROHIT, Ajay , HARRIS, Thomas, D. , ROBINSON, Simon, P. , YU, Ming , CASEBIER, David, S. , HU, Carol, Hui , BROEKEMA, Matthias , ONTHANK, David, C.
IPC分类号： C07D233/44
CPC分类号： A61K51/0459 , A61K51/04 , A61K51/041 , A61K51/0453 , A61K51/0497 , C07B2200/05 , C07C217/70 , C07C257/14 , C07C279/04 , C07C279/06 , C07C279/08 , C07C279/12 , C07C279/14 , C07C281/18 , C07D209/14 , C07D233/46
摘要： The present invention relates to systems, compositions, and methods for the synthesis and use of imaging agents, or precursors thereof. An imaging agent precursor may be converted to an imaging agent using the methods described herein. In some cases, the imaging agent is enriched in 18 F. In some cases, an imaging agent may be used to image an area of interest in a subject, including, but not limited to, the heart, cardiovascular system, cardiac vessels, brain, and other organs. In some embodiments, methods and compositions for assessing perfusion and innervation mismatch in a portion of a subject are provided.
摘要翻译：本发明涉及用于合成和使用成像剂或其前体的体系，组合物和方法。成像剂前体可以使用本文所述的方法转化成成像剂。在一些情况下，成像剂富集在18F中。在一些情况下，成像剂可用于对受试者感兴趣的区域成像，包括但不限于心脏，心血管系统，心脏血管，脑，等器官。在一些实施例中，提供了用于评估受试者的一部分中的灌注和神经支配失配的方法和组合物。

25. 发明申请

WO2005072082A3 2-GUANIDINYLIMIDAZOLIDINEDIONE COMPOUNDS AND METHODS OF MAKING AND USING THEREOF 审中-公开
标题翻译： 2-胍基二咪唑啉化合物及其制备和使用方法
公开(公告)号：WO2005072082A3
公开(公告)日：2005-12-22
申请号：PCT/US2004038909
申请日：2004-11-19
申请人： US ARMY MED RES MAT COMMAND , LIN AI J , ZHANG QUAN , GUAN JIAN , MILHOUS WILBUR K
发明人： LIN AI J , ZHANG QUAN , GUAN JIAN , MILHOUS WILBUR K
IPC分类号： A61K31/4168 , A61K31/4178 , C07D233/44 , C07D233/54 , C07D405/12
CPC分类号： C07D233/96 , C07D233/54 , C07D405/12
摘要： Disclosed herein are 2-guanidinylimidazolidinedione compounds having the structural Formula A or B wherein R 1 and R 2 are each independently a hydrogen, halogen, alkyl, alkoxyl, amino, alkylamino or aralkyl, and wherein R 3 is an alkyl, cycloalkyl, heterocycloalkyl, acyl, aryl, heteroaryl, alkylaryl, sulfonyl, alkylsulfonyl, and pharmaceutically acceptable salts thereof, and methods of making thereof. Also disclosed are methods of treating, preventing, or inhibiting malaria with the 2-guanidinylimidazolidinedione compounds, and pharmaceutical compositions comprising the 2-guanidinylimidazolidinedione compounds, and kits.
摘要翻译：本文公开了具有结构式A或B的2-胍基咪唑烷二酮化合物，其中R 1和R 2各自独立地为氢，卤素，烷基，烷氧基，氨基，烷基氨基或芳烷基，其中R 3是烷基，环烷基，杂环烷基，酰基，芳基，杂芳基，烷基芳基，磺酰基，烷基磺酰基及其药学上可接受的盐，及其制备方法。还公开了用2-胍基咪唑烷二酮化合物治疗，预防或抑制疟疾的方法，以及包含2-胍基脒基咪唑烷二酮化合物的药物组合物和试剂盒。

26. 发明申请

WO2005072082A2 2-GUANIDINYLIMIDAZOLIDINEDIONE COMPOUNDS AND METHODS OF MAKING AND USING THEREOF 审中-公开
标题翻译： 2-胍基二咪唑啉化合物及其制备和使用方法
公开(公告)号：WO2005072082A2
公开(公告)日：2005-08-11
申请号：PCT/US2004/038909
申请日：2004-11-19
申请人： U.S. ARMY MEDICAL RESEARCH AND MATERIEL COMMAND , LIN, Ai J. , ZHANG, Quan , GUAN, Jian , MILHOUS, Wilbur K.
发明人： LIN, Ai J. , ZHANG, Quan , GUAN, Jian , MILHOUS, Wilbur K.
IPC分类号： A61K31/4168 , A61K31/4178 , C07D233/44 , C07D233/54 , C07D405/12
CPC分类号： C07D233/96 , C07D233/54 , C07D405/12
摘要： Disclosed herein are 2-guanidinylimidazolidinedione compounds having the structural Formula A or B wherein R 1 and R 2 are each independently a hydrogen, halogen, alkyl, alkoxyl, amino, alkylamino or aralkyl, and wherein R 3 is an alkyl, cycloalkyl, heterocycloalkyl, acyl, aryl, heteroaryl, alkylaryl, sulfonyl, alkylsulfonyl, and pharmaceutically acceptable salts thereof, and methods of making thereof. Also disclosed are methods of treating, preventing, or inhibiting malaria with the 2-guanidinylimidazolidinedione compounds, and pharmaceutical compositions comprising the 2-guanidinylimidazolidinedione compounds, and kits.
摘要翻译：本文公开了具有结构式A或B的2-胍基咪唑烷二酮化合物，其中R 1和R 2各自独立地为氢，卤素，烷基，烷氧基，氨基，烷基氨基或芳烷基，并且其中R 3为烷基，环烷基，杂环烷基，酰基，芳基，杂芳基，烷基芳基，磺酰基，烷基磺酰基及其药学上可接受的盐及其制备方法。还公开了用2-胍基咪唑烷二酮化合物治疗，预防或抑制疟疾的方法，以及包含2-胍基脒基咪唑烷二酮化合物的药物组合物和试剂盒。

27. 发明申请

WO98046571A1 METHODS FOR SYNTHESIZING 2-SUBSTITUTED IMIDAZOLES 审中-公开
标题翻译：用于合成2-取代的咪唑的方法
公开(公告)号：WO98046571A1
公开(公告)日：1998-10-22
申请号：PCT/US1998/007614
申请日：1998-04-17
IPC分类号： C07D233/66 , C07D401/04 , C07D401/12 , C07D233/44 , C07D233/46 , C07D233/48 , C07D401/00 , C07D405/00 , C07D409/00 , C07D411/00 , C07D413/00 , C07D417/00 , C07D419/00 , C07D421/00
CPC分类号： C07D401/04 , C07D401/12
摘要： The present invention is a method of preparing 2-substituted imidazoles from readily available imidazoles having a leaving group in the 2-position, by alkylating the imidazole under mild conditions to afford a 3-N-alkylated imidazolium salt; and coupling the imidazolium salt with a nucleophile also under mild conditions to afford a 2-substituted 3-N-alkylated imidazolium salt. The reaction product can optionally be isolated and purified. The 2-substituted 3-N-alkylated imidazolium salt is hydrolyzed to afford a 2-substituted imidazole. Alternatively, the imidazole is coupled with a nucleophile in the presence of fluoride ion to provide a 2-substituted imidazole.
摘要翻译：本发明是一种通过在温和条件下使咪唑烷基化得到3-N-烷基化的咪唑盐，从容易得到的具有2-位离去基团的咪唑制备2-取代咪唑的方法; 并且在温和条件下将咪唑鎓盐与亲核试剂偶联以得到2-取代的3-N-烷基化的咪唑鎓盐。反应产物可任选地被分离和纯化。将2-取代的3-N-烷基化咪唑鎓盐水解，得到2-取代的咪唑。或者，咪唑在存在氟离子的情况下与亲核试剂偶联以提供2-取代的咪唑。

28. 发明申请

WO1997022593A1 NOVEL 5-AMINO-3-CYANO-4-ETHYLSULFINYL-1-PHENYL-PYRAZOLE COMPOUNDS AND THEIR USE AS PESTICIDES 审中-公开
标题翻译：新型5-氨基-3-氰基-4-乙酰氧基-1-苯基 - 吡唑化合物及其作为农药的用途
公开(公告)号：WO1997022593A1
公开(公告)日：1997-06-26
申请号：PCT/EP1996005696
申请日：1996-12-19
申请人： RHONE-POULENC AGROCHIMIE
发明人： RHONE-POULENC AGROCHIMIE , HAAS, Charles, Lee , PILATO, Michael, Thomas , WU, Tai-Teh
IPC分类号： C07D233/44
CPC分类号： C07D231/38 , A01N43/56 , C07D231/44 , A01N2300/00 , A01N43/30
摘要： The invention relates to 1-arylpyrazoles of general formula (I), wherein X is chlorine or bromine; Y is trifluoromethyl or trifluoromethoxy and R1 is hydrogen, methyl or ethyl, and to their use as pesticides.
摘要翻译：本发明涉及通式（I）的1-芳基吡唑，其中X为氯或溴; Y为三氟甲基或三氟甲氧基，R 1为氢，甲基或乙基，并用作农药。

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