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21. 发明申请

WO2002090314A1 PYRUVATE DERIVATIVES 审中-公开
标题翻译：吡咯烷酮衍生物
公开(公告)号：WO2002090314A1
公开(公告)日：2002-11-14
申请号：PCT/US2002/014057
申请日：2002-05-03
申请人： GALILEO LABORATORIES, INC. , WANG, Bing , MILLER, Guy , FLAIM, Stephen, F. , DEL BALZO, Ughetta , ZHANG, Wei , JANAGANI, Satyanarayana , SONG, Jingao
发明人： WANG, Bing , MILLER, Guy , FLAIM, Stephen, F. , DEL BALZO, Ughetta , ZHANG, Wei , JANAGANI, Satyanarayana , SONG, Jingao
IPC分类号： C07C69/66
CPC分类号： C07D213/30 , A61K31/12 , A61K31/16 , A61K31/215 , A61K31/223 , A61K38/00 , C07C249/12 , C07C319/20 , C07C323/60 , C07D207/16 , C07D207/22 , C07D207/24 , C07D211/62 , C07D211/74 , C07D211/78 , C07D217/04 , C07D233/42 , C07D233/64 , C07D233/84 , C07D235/28 , C07D239/78 , C07D249/14 , C07D271/113 , C07D277/16 , C07D277/74 , C07D279/12 , C07D285/125 , C07D285/135 , C07D295/13 , C07D295/15 , C07D295/185 , C07D339/08 , C07D345/00 , C07D405/12 , C07D473/38 , C07K5/0215 , C07K5/0819 , C07C323/57 , C07C251/60
摘要： Certain known and novel pyruvate derivatives are particularly active in restoring or preserving metabolic integrity in oxidatively competent cells that have been subjected to oxygen deprivation. These pyruvate-derived compounds include, but are not limited to oximes, amides, pyruvate analogues, modified pyruvate analogues, esters of pyruvate (e.g., polyol-pyruvate esters, pyruvate thioesters, glycerol-pyruvate esters and dihydroxyacetone-pyruvate esters). Such pyruvate derivatives (including single tautomers, single stereoisomers and mixtures of tautomers and/or stereoisomers, and the pharmaceutically acceptable salts thereof) are useful in the manufacture of pharmaceutical compositions for treating a number of conditions characterized by oxidative stress.
摘要翻译：某些已知和新颖的丙酮酸衍生物在恢复或保持已经遭受氧剥夺的氧化感受态细胞中的代谢完整性方面特别有活性。这些丙酮酸衍生化合物包括但不限于肟，酰胺，丙酮酸盐类似物，改性丙酮酸盐类似物，丙酮酸酯（例如多元醇 - 丙酮酸酯，丙酮酸硫酯，甘油 - 丙酮酸酯和二羟基丙酮 - 丙酮酸酯）。这样的丙酮酸衍生物（包括单互变异构体，单立体异构体和互变异构体和/或立体异构体的混合物及其药学上可接受的盐）可用于制备用于治疗以氧化应激为特征的许多病症的药物组合物。

22. 发明申请

WO00052530A1 OXIME DERIVATIVES AND THE USE THEREOF AS PHOTOINITIATORS 审中-公开
标题翻译： OXIME衍生物及其作为光敏剂的用途
公开(公告)号：WO00052530A1
公开(公告)日：2000-09-08
申请号：PCT/EP2000/001404
申请日：2000-02-21
IPC分类号： C07C309/66 , C07C309/73 , C07C323/57 , C07C381/00 , C07D307/54 , C07D307/66 , C07D333/36 , C07D339/08 , C07F9/09 , C07F9/32 , C07F9/6553 , C08F2/50 , G03F7/031
CPC分类号： G03F7/031 , B33Y70/00 , C07C309/66 , C07C309/73 , C07C323/57 , C07C381/00 , C07D307/66 , C07D333/36 , C07D339/08 , C07F9/097 , C07F9/655345 , C08F2/50 , Y10S430/12 , Y10S430/123
摘要： Radically photopolymerizable compositions comprising (a) at least one ethylenically unsaturated photopolymerizable compound; (b) as photoinitiator, at least one compound of formulae (I, II, III, IV, V and/or VI), wherein m is 0 or 1; n is 0, 1, 2 or 3; x is 1 or 2; R1 is inter alia phenyl, naphthyl, anthracyl or phenanthryl, a heteroaryl radical, C2-C12alkenyl, C4-C8cycloalkenyl, or C6-C12bicycloalkenyl; R'1 is inter alia C2-C12alkylene, or phenylene; R2 has one of the meanings of R1 or inter alia is phenyl; y is 1 or 2; R3 if x is 1 inter alia is C1-C18alkylsulfonyl, or phenyl-C1-C3alkylsulfonyl, R3 if x is 2, is for example C2-C12alkylenedisulfonyl; R4 and R5 inter alia are hydrogen, halogen, or C1-C8alkyl; R6, R7, R8 inter alia are hydrogen, R26Y-, or phenyl; R9 inter alia is C5-C8cycloalkyl, or phenyl; A is for example -S-, -O-, or -NR10- ; Q is C1-C8-alkylene optionally interrupted by -O-; X is -O- or -NR9-; R10 inter alia is hydrogen, or phenyl; and (c) at least one coinitiator; are especially suitable for the preparation of colour filter systems.
摘要翻译：自由基光聚合组合物，其包含（a）至少一种烯属不饱和光聚合化合物; （b）作为光引发剂，至少一种式（I，II，III，IV，V和/或VI）的化合物，其中m为0或1; n为0,1,2或3; x为1或2; R 1特别是苯基，萘基，蒽基或菲基，杂芳基，C 2 -C 12烯基，C 4 -C 8环烯基或C 6 -C 12双环烯基; R'1特别是C 2 -C 12亚烷基或亚苯基; R2具有R1的含义之一，特别是苯基; y为1或2; 如果x是1，则R3如果是C 1 -C 18烷基磺酰基，或苯基-C 1 -C 3烷基磺酰基，如果x是2，则R 3是例如C 2 -C 12亚烷基二磺酰基; R4和R5尤其是氢，卤素或C1-C8烷基; R6，R7，R8特别是氢，R26Y-或苯基; R9尤其是C5-C8环烷基或苯基; A是例如-S-，-O-或-NR 10 - ; Q是任选被-O-间隔的C1-C8-亚烷基; X是-O-或-NR 9 - ; R 10尤其是氢或苯基; 和（c）至少一种共引发剂; 特别适用于制备滤色器系统。

23. 发明授权

US09682929B2 Metalloprotease inhibitors, methods for producing same, and therapeutics uses thereof 有权
公开(公告)号：US09682929B2
公开(公告)日：2017-06-20
申请号：US14915807
申请日：2014-09-02
申请人： Centre National de la Recherche Scientifique-CNRS , Universite de Reims Champagne-Ardenne
发明人： Samir Bouzbouz , Xavier Pannecoucke , Azzaq Belaaouaj , Laurette Malleret , Clement Denhez , Dominique Guillaume
IPC分类号： C07C237/22 , C07C319/12 , C07D231/22 , C07C231/10 , C07C235/34 , C07C231/12 , C07C69/533 , C07C67/31 , C07C323/57 , C07C235/28 , C07C323/60 , C07C67/14 , C07C69/732 , C07C323/59 , C07C67/343
CPC分类号： C07C319/12 , C07C67/14 , C07C67/31 , C07C67/343 , C07C69/533 , C07C69/732 , C07C231/10 , C07C231/12 , C07C235/28 , C07C235/34 , C07C237/22 , C07C323/57 , C07C323/59 , C07C323/60 , C07C2601/14 , C07D231/22 , C07C69/54
摘要： The invention relates to new α-vinyl carbonylated compounds corresponding to general formula (I), wherein R1, R2,R3, R4, R5 and Y are as defined in claim 1, their isomers, their diastereoisomers and acid addition salts or a pharmaceutically acceptable base. The invention also relates to a method for producing said compounds (I). It further relates to the use of said compound (I) as selective metalloprotease inhibitors, especially matrix metalloproteases 12 (MMP-12) and/or 9 (MMP-9). The compounds (I) are particularly useful for the prevention and/or treatment of chronic obstructive pulmonary disease (COPD), particularly emphysema induced by cigarette smoke.

24. 发明申请

US20160200676A1 METALLOPROTEASE INHIBITORS, METHODS FOR PRODUCING SAME, AND THERAPEUTIC USES THEREOF 有权
标题翻译：金属蛋白酶抑制剂，其生产方法及其治疗用途
公开(公告)号：US20160200676A1
公开(公告)日：2016-07-14
申请号：US14915807
申请日：2014-09-02
申请人： CENTRE NATIONAL DE LA RECHERCHE SCIENTIFIQUE - CNRS , UNIVERSITE DE REIMS CHAMPAGNE-ARDENNE
发明人： Samir Bouzbouz , Xavier Pannecoucke , Azzaq Belaaouaj , Laurette Malleret , Clement Denhez , Dominique Guillaume
IPC分类号： C07C319/12 , C07C235/34 , C07D231/22 , C07C67/31 , C07C69/533 , C07C231/10 , C07C231/12 , C07C67/14 , C07C235/28 , C07C323/57
CPC分类号： C07C319/12 , C07C67/14 , C07C67/31 , C07C67/343 , C07C69/533 , C07C69/732 , C07C231/10 , C07C231/12 , C07C235/28 , C07C235/34 , C07C237/22 , C07C323/57 , C07C323/59 , C07C323/60 , C07C2601/14 , C07D231/22 , C07C69/54
摘要： The invention relates to new α-vinyl carbonylated compounds corresponding to general formula (I), wherein R1, R2, R3, R4, R5 and Y are as defined in claim 1, their isomers, their diastereoisomers and acid addition salts or a pharmaceutically acceptable base. The invention also relates to a method for producing said compounds (I). It further relates to the use of said compounds (I) as selective metalloprotease inhibitors, especially matrix metalloproteases 12 (MMP-12) and/or 9 (MMP-9). The compounds (I) are particularly useful for the prevention and/or treatment of chronic obstructive pulmonary disease (COPD), particularly emphysema induced by cigarette smoke.
摘要翻译：本发明涉及对应于通式（I）的新的α-乙烯基羰基化化合物，其中R1，R2，R3，R4，R5和Y如权利要求1所定义，它们的异构体，它们的非对映异构体和酸加成盐或药学上可接受的基础。本发明还涉及一种生产所述化合物（I）的方法。它还涉及所述化合物（I）作为选择性金属蛋白酶抑制剂，特别是基质金属蛋白酶12（MMP-12）和/或9（MMP-9）的用途。化合物（I）特别可用于预防和/或治疗慢性阻塞性肺疾病（COPD），特别是由香烟烟雾引起的肺气肿。

25. 发明申请

US20150133470A1 SUBSTITUTED N-ACETYL-L-CYSTEINE DERIVATIVES AND RELATED COMPOUNDS 有权
标题翻译：取代的N-乙酰基-L-胞嘧啶衍生物及相关化合物
公开(公告)号：US20150133470A1
公开(公告)日：2015-05-14
申请号：US14535855
申请日：2014-11-07
申请人： Promentis Pharmaceuticals, Inc.
发明人： Michael Neary , James Nieman , Steven Tanis , Daniel Lawton , Garry Smith
IPC分类号： C07D277/14 , C07D241/08 , C07C323/58 , C07C323/59 , C07C327/32 , C07C329/06
CPC分类号： C07D277/08 , A61K31/165 , A61K31/265 , A61K31/426 , A61K31/513 , C07C323/57 , C07C323/58 , C07C323/59 , C07C323/60 , C07C327/26 , C07C327/32 , C07C327/34 , C07C329/06 , C07D241/08 , C07D277/14 , C07D327/04
摘要： Novel substituted N-acetyl-L-cysteine (NAC) derivatives and related compounds and methods of using these compounds for the treatment of diseases and/or conditions, including but not limited to diseases and/or conditions of, or involving, the Central Nervous System (CNS), including schizophrenia adrenoleukodystrophy, mitochondrial diseases (e.g. Leigh syndrome, Alpers' disease, and MELAS), Huntington's disease, trichotillomania, HIV-associated neurocognitive disorder, hypoxic-ischemic encephalopathy, drug craving, and drug addiction.
摘要翻译：新型取代的N-乙酰基-L-半胱氨酸（NAC）衍生物和相关化合物以及使用这些化合物治疗疾病和/或病症的方法，包括但不限于中枢神经的疾病和/或病症或涉及中枢神经系统（CNS），包括精神分裂症肾上腺脑白质营养不良，线粒体疾病（例如Leigh综合征，阿尔卑斯病和MELAS），亨廷顿舞蹈病，拔毛病，艾滋病毒相关神经认知障碍，缺氧缺血性脑病，药物渴求和药物成瘾。

27. 发明申请

US20030013657A1 Pyruvate derivatives 失效
标题翻译：丙酮酸衍生物
公开(公告)号：US20030013657A1
公开(公告)日：2003-01-16
申请号：US10138938
申请日：2002-05-03
发明人： Bing Wang , Guy Miller , Satyanarayana Janagani
IPC分类号： A61K038/08 , A61K038/06 , A61K031/7076 , A61K031/7072 , A61K031/44 , A61K031/401 , A61K031/198
CPC分类号： C07D213/30 , A61K31/12 , A61K31/16 , A61K31/215 , A61K31/223 , A61K38/00 , C07C249/12 , C07C319/20 , C07C323/60 , C07D207/16 , C07D207/22 , C07D207/24 , C07D211/62 , C07D211/74 , C07D211/78 , C07D217/04 , C07D233/42 , C07D233/64 , C07D233/84 , C07D235/28 , C07D239/78 , C07D249/14 , C07D271/113 , C07D277/16 , C07D277/74 , C07D279/12 , C07D285/125 , C07D285/135 , C07D295/13 , C07D295/15 , C07D295/185 , C07D339/08 , C07D345/00 , C07D405/12 , C07D473/38 , C07K5/0215 , C07K5/0819 , C07C323/57 , C07C251/60
摘要： Certain known and novel pyruvate derivatives are particularly active in restoring or preserving metabolic integrity in oxidatively competent cells that have been subjected to oxygen deprivation. These pyruvate-derived compounds include, but are not limited to oximes, amides, pyruvate analogues, modified pyruvate analogues, esters of pyruvate (e.g., polyol-pyruvate esters, pyruvate thioesters, glycerol-pyruvate esters and dihydroxyacetone-pyruvate esters). Such pyruvate derivatives (including single tautomers, single stereoisomers and mixtures of tautomers and/or stereoisomers, and the pharmaceutically acceptable salts thereof) are useful in the manufacture of pharmaceutical compositions for treating a number of conditions characterized by oxidative stress.
摘要翻译：某些已知和新颖的丙酮酸衍生物在恢复或保持已经遭受氧剥夺的氧化感受态细胞中的代谢完整性方面特别有活性。这些丙酮酸衍生化合物包括但不限于肟，酰胺，丙酮酸盐类似物，改性丙酮酸盐类似物，丙酮酸酯（例如多元醇 - 丙酮酸酯，丙酮酸硫酯，甘油 - 丙酮酸酯和二羟基丙酮 - 丙酮酸酯）。这种丙酮酸衍生物（包括单互变异构体，单立体异构体和互变异构体和/或立体异构体的混合物及其药学上可接受的盐）可用于制备用于治疗以氧化应激为特征的许多病症的药物组合物。

28. 发明授权

US5473100A Hydroxamic acid derivative 失效
标题翻译：羟肟酸衍生物
公开(公告)号：US5473100A
公开(公告)日：1995-12-05
申请号：US409709
申请日：1995-03-24
申请人： Yasuo Isomura , Seijiro Akamatsu , Toru Yoden , Masafumi Kudou , Akira Suga
发明人： Yasuo Isomura , Seijiro Akamatsu , Toru Yoden , Masafumi Kudou , Akira Suga
IPC分类号： A61K31/165 , A61K31/19 , A61K31/215 , A61K31/265 , A61P1/02 , A61P27/02 , A61P29/00 , A61P43/00 , C07C237/22 , C07C259/06 , C07C323/57 , C07C323/60 , C07C327/30 , C07C327/32 , C07C327/34 , C07C259/04
CPC分类号： C07C259/06 , C07C237/22 , C07C323/57 , C07C323/60 , C07C327/30 , C07C327/32 , C07C327/34
摘要： ##STR1## A compound represented by general formula (I), a pharmaceutical composition containing same, a process for the production thereof, and an intermediate therefor. In formula (I) R
1 represents lower alkyl which may be substituted by a substituent selected from the group consisting of mercapto, lower alkylthio, arylthio and lower acylthio; R
2 , R
3 and R
4 may be the same or different from one another and each represents lower alkyl; X represents oxygen or sulfur; and Y represents a single bond or lower alkylene. The compound (I) has a matrix metalloprotease inhibitory activity and is useful for preventing and treating diseases caused by the progress of connective tissue breakage.
摘要翻译：由通式（I）表示的化合物，含有该化合物的药物组合物，其制备方法及其中间体。在式（I）中，R 1表示可以被选自巯基，低级烷硫基，芳硫基和低级酰硫基的取代基取代的低级烷基; R2，R3和R4可以相同或不同，各自表示低级烷基; X表示氧或硫; Y表示单键或低级亚烷基。化合物（I）具有基质金属蛋白酶抑制活性，可用于预防和治疗由结缔组织破裂进展引起的疾病。

29. 发明申请

US20150133544A1 ETHYL (2R)-2-ACETAMIDO-3-(4-METHYLBENZOYLSULFANYL)PROPANOATE AND USES THEREOF 有权
标题翻译：乙酰（2R）-2-乙酰氨基-3-（4-甲基苯甲酰基）丙酸酯及其用途
公开(公告)号：US20150133544A1
公开(公告)日：2015-05-14
申请号：US14535953
申请日：2014-11-07
申请人： Promentis Pharmaceuticals, Inc.
发明人： Michael Neary , James Nieman , Steven Tanis , Daniel Lawton
IPC分类号： C07C327/34
CPC分类号： C07D277/08 , A61K31/165 , A61K31/265 , A61K31/426 , A61K31/513 , C07C323/57 , C07C323/58 , C07C323/59 , C07C323/60 , C07C327/26 , C07C327/32 , C07C327/34 , C07C329/06 , C07D241/08 , C07D277/14 , C07D327/04
摘要： A novel substituted N-acetyl-L-cysteine (NAC) derivative and methods of using this compound for the treatment of diseases and/or conditions, including but not limited to diseases and/or conditions of, or involving, the Central Nervous System (CNS), including schizophrenia adrenoleukodystrophy, mitochondrial diseases (e.g. Leigh syndrome, Alpers' disease, and MELAS), Huntington's disease, trichotillomania, HIV-associated neurocognitive disorder, hypoxic-ischemic encephalopathy, drug craving, and drug addiction.
摘要翻译：新型取代的N-乙酰基-L-半胱氨酸（NAC）衍生物和使用该化合物治疗疾病和/或病症的方法，包括但不限于中枢神经系统的疾病和/或病症或涉及中枢神经系统 CNS），包括精神分裂症肾上腺脑白质营养不良，线粒体疾病（例如Leigh综合征，阿尔卑斯病和MELAS），亨廷顿病，头痛性痴呆，HIV相关神经认知障碍，缺氧缺血性脑病，药物渴求和药物成瘾。

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