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1. 发明申请

WO2020243650A1 DEUTERATED ANALOGS OF D-SERINE AND USES THEREOF 审中-公开
公开(公告)号：WO2020243650A1
公开(公告)日：2020-12-03
申请号：PCT/US2020/035429
申请日：2020-05-29
申请人： CONCERT PHARMACEUTICALS, INC. , DOLLER, Dario , BRUMMEL, Christopher L. , LIU, Julie F. , TUNG, Roger D. , WONG, Darren H. , PETRYSHEN, Tracey L. , HURST, Raymond S.
发明人： DOLLER, Dario , BRUMMEL, Christopher L. , LIU, Julie F. , TUNG, Roger D. , WONG, Darren H. , PETRYSHEN, Tracey L. , HURST, Raymond S.
IPC分类号： A61K31/198 , A61K38/00 , C07B59/00 , A61P25/16
摘要： This disclosure relates to deuterated D-serine, pharmaceutically acceptable salts thereof, analogs and prodrugs thereof, pharmaceutical compositions thereof, and methods of use.

2. 发明申请

WO2020092604A1 DEUTERATED PITOLISANT 审中-公开
公开(公告)号：WO2020092604A1
公开(公告)日：2020-05-07
申请号：PCT/US2019/058909
申请日：2019-10-30
申请人： CONCERT PHARMACEUTICALS, INC. , TUNG, Roger D. , LIU, Julie F. , HURST, Raymond S.
发明人： TUNG, Roger D. , LIU, Julie F. , HURST, Raymond S.
IPC分类号： A61K31/137 , A61K31/4402
摘要： This invention also provides compound of Formula (I) including pharmaceutical compositions comprising a compound of Formula (I) and a pharmaceutically acceptable carrier. This invention also provides the use of such compounds and compositions in methods of treating diseases and conditions that are beneficially treated by administering pitolisant. Some exemplary embodiments include a method of treating a disease or condition selected from narcolepsy, daytime sleepiness (particularly in subjects suffering from Parkinson's disease or obstructive sleep apnea syndrome), and cognitive defects in psychiatric conditions, the method comprising the step of administering to a subject in need thereof a pharmaceutically acceptable composition of the present invention.

3. 发明申请

WO2012122028A3 PYRAZINOISOQUINOLINE COMPOUNDS 审中-公开
标题翻译：吡咯烷酮化合物
公开(公告)号：WO2012122028A3
公开(公告)日：2013-08-15
申请号：PCT/US2012027528
申请日：2012-03-02
申请人： CONCERT PHARMACEUTICALS INC , LIU JULIE F
发明人： LIU JULIE F
IPC分类号： A61K31/502
CPC分类号： C07D471/04 , A61K31/4184 , A61K31/4985 , C07B59/002
摘要： This invention in one embodiment is directed to a compound of Formula (la); where the designation (R) indicates that the designated carbon has the (R) stereochemistry; and wherein Z1 is hydrogen or fluorine; Z2 is hydrogen, deuterium, or fluorine; Z3 is deuterium; Z4 is fluorine; m is an integer from 0 to 10; n is an integer from 0 to 2; provided that: the sum of m + n does not exceed 10; and when both Z1 and Z2 are hydrogen, the sum of m + n is greater than 0, and pharmaceutically acceptable salts thereof. This invention also provides compositions comprising one or more compounds of this invention and a carrier and the use of the disclosed compounds and compositions in methods of treating diseases and conditions that are beneficially treated by administering an antihelminthic agent, such as praziquantel.
摘要翻译：本发明在一个实施方案中涉及式（Ia）的化合物; 其中指定（R）表示指定的碳具有（R）立体化学; 并且其中Z1是氢或氟; Z2是氢，氘或氟; Z3是氘; Z4是氟; m为0〜10的整数; n为0〜2的整数; 条件是：m + n的和不超过10; 并且当Z1和Z2均为氢时，m + n的和大于0，以及其药学上可接受的盐。本发明还提供包含一种或多种本发明化合物和载体的组合物，以及所述化合物和组合物在治疗通过施用抗栓剂如吡喹酮有益治疗的疾病和病症的方法中的用途。

4. 发明申请

WO2011028922A1 SUBSTITUTED XANTHINE DERIVATIVES 审中-公开
标题翻译：取代的XANTHINE衍生物
公开(公告)号：WO2011028922A1
公开(公告)日：2011-03-10
申请号：PCT/US2010/047708
申请日：2010-09-02
申请人： CONCERT PHARMACEUTICALS, INC. , TUNG, Roger D. , LIU, Julie F. , HARBESON, Scott L.
发明人： TUNG, Roger D. , LIU, Julie F. , HARBESON, Scott L.
IPC分类号： A01N43/90 , A61K31/522
CPC分类号： C07D473/04
摘要： This invention relates to novel compounds that are substituted xanthine derivatives and pharmaceutically acceptable salts thereof. For example, this invention relates to novel substituted xanthine derivatives that are derivatives of pentoxifylline. This invention also provides compositions comprising one or more compounds of this invention and a carrier and the use of the disclosed compounds and compositions in methods of treating diseases and conditions for which pentoxifylline and related compounds are beneficial.
摘要翻译：本发明涉及作为取代黄嘌呤衍生物的新化合物及其药学上可接受的盐。例如，本发明涉及作为己酮可可碱衍生物的新型取代黄嘌呤衍生物。本发明还提供包含一种或多种本发明化合物和载体的组合物，以及所述化合物和组合物在治疗己酮可可碱和相关化合物有益的疾病和病症的方法中的用途。

5. 发明申请

WO2011028835A1 SUBSTITUTED XANTHINE DERIVATIVES 审中-公开
标题翻译：取代的黄嘌呤衍生物
公开(公告)号：WO2011028835A1
公开(公告)日：2011-03-10
申请号：PCT/US2010/047574
申请日：2010-09-01
申请人： CONCERT PHARMACEUTICALS, INC. , TUNG, Roger, D. , LIU, Julie, F. , HARBESON, Scott, L.
发明人： TUNG, Roger, D. , LIU, Julie, F. , HARBESON, Scott, L.
IPC分类号： A01N43/90 , A61K31/522
CPC分类号： C07D473/04 , C07D473/06
摘要： This invention relates to novel compounds that are substituted xanthine derivatives and pharmaceutically acceptable salts thereof. For example, this invention relates to novel substituted xanthine derivatives that are derivatives of pentoxifylline. This invention also provides compositions comprising one or more compounds of this invention and a carrier and the use of the disclosed compounds and compositions in methods of treating diseases and conditions for which pentoxifylline and related compounds are beneficial.
摘要翻译：本发明涉及取代的黄嘌呤衍生物及其药学上可接受的盐的新化合物。例如，本发明涉及作为己酮可可碱衍生物的新型取代的黄嘌呤衍生物。本发明还提供了包含一种或多种本发明化合物和载体的组合物，以及所公开的化合物和组合物在治疗己酮可可碱和相关化合物有益的疾病和病症的方法中的用途。

6. 发明申请

WO2010107791A4 PYRAZINOISOQUINOLINE COMPOUNDS 审中-公开
标题翻译：吡咯烷酮化合物
公开(公告)号：WO2010107791A4
公开(公告)日：2011-01-13
申请号：PCT/US2010027476
申请日：2010-03-16
申请人： CONCERT PHARMACEUTICALS INC , LIU JULIE F , TUNG ROGER , HARBESON SCOTT L
发明人： LIU JULIE F
IPC分类号： C07D471/04 , A61K31/4985
CPC分类号： C07D471/04 , A61K31/4184 , A61K31/4985 , A61K45/06 , A61K2300/00
摘要： This invention relates to novel compounds that are pyrazinoisoquinoline derivatives, and pharmaceutically acceptable salts thereof. More specifically, this invention relates to novel pyrazinoisoquinoline derivatives that are derivatives of praziquantel. This invention also provides compositions comprising one or more compounds of this invention and a carrier and the use of the disclosed compounds and compositions in methods of treating diseases and conditions that are beneficially treated by administering an antihelminthic agent, such as praziquantel.
摘要翻译：本发明涉及吡嗪并异喹啉衍生物的新化合物及其药学上可接受的盐。更具体地，本发明涉及作为吡喹酮衍生物的新型吡嗪异喹啉衍生物。本发明还提供包含一种或多种本发明化合物和载体的组合物，以及所述化合物和组合物在治疗通过施用抗栓剂如吡喹酮有益治疗的疾病和病症的方法中的用途。

7. 发明申请

WO2010147922A1 DEUTERATED I SOINDOLINE- I, 3-DIONE DERIVATIVES AS PDE4 AND TNF-ALPHA INHIBITORS 审中-公开
标题翻译：作为PDE4和TNF-ALPHA抑制剂去除I二氢吲哚-1-酮，3-二酮衍生物
公开(公告)号：WO2010147922A1
公开(公告)日：2010-12-23
申请号：PCT/US2010/038577
申请日：2010-06-15
申请人： CONCERT PHARMACEUTICALS, INC. , LIU, Julie, F.
发明人： LIU, Julie, F.
IPC分类号： C07D209/46 , C07D209/48 , C07D405/12 , A61K31/4035 , A61P17/06
CPC分类号： C07D209/48 , C07B59/002 , C07B2200/05 , C07D207/404 , C07D209/46 , C07D405/12
摘要： This invention relates to novel substituted isoindoline-l,3-dione derivatives' of formula I and pharmaceutically acceptable salts thereof. More specifically, the invention relates to novel substituted isoindoline-l,3-dione derivatives that are analogues of apremilast. This invention also provides compositions comprising a compound of this invention and a carrier and the use of disclosed compounds and compositions in methods of treating diseases and conditions that are beneficially treated by administering apremilast.
摘要翻译：本发明涉及式I的新型取代的异二氢吲哚-1,3-二酮衍生物及其药学上可接受的盐。更具体地，本发明涉及作为去甲生物的类似物的新的取代的异二氢吲哚-1,3-二酮衍生物。本发明还提供了包含本发明化合物和载体的组合物，以及所述化合物和组合物在治疗通过施用去甲苯磺酸酯有益治疗的疾病和病症的方法中的用途。

8. 发明申请

WO2010036773A1 DEUTERATED L-ARYL-2 -AMINOMETHYL CYCLOPROPANE CARBOXYAMIDE DERIVATIVES 审中-公开
标题翻译：去离子L-芳基-2-氨基甲酰基环丙烷羧酸衍生物
公开(公告)号：WO2010036773A1
公开(公告)日：2010-04-01
申请号：PCT/US2009/058173
申请日：2009-09-24
申请人： CONCERT PHARMACEUTICALS, INC. , LIU, Julie, F.
发明人： LIU, Julie, F.
IPC分类号： C07C237/24 , A61K31/165 , A61P25/24
CPC分类号： C07C237/24 , C07C2601/02
摘要： This invention relates to novel compounds that are 1 -aryl-2-aminomethyl cyclopropane carboxyamide derivatives and pharmaceutically acceptable salts thereof. More specifically, this invention relates to novel 1 -aryl-2-aminomethyl cyclopropane carboxyamide derivatives that are derivatives of milnacipran. This invention also provides pyrogen free compositions comprising one or more compounds of the invention and a carrier, and the use of the disclosed compounds and compositions in methods of treating diseases and conditions that are beneficially treated by administering a πorepinephrine/serotonin reuptake inhibitor (NSRI), such us milnacipran.
摘要翻译：本发明涉及1-芳基-2-氨基甲基环丙烷羧酰胺衍生物及其药学上可接受的盐的新化合物。更具体地，本发明涉及作为米那普兰衍生物的新型1-芳基-2-氨基甲基环丙烷羧酰胺衍生物。本发明还提供无热原组合物，其包含一种或多种本发明化合物和载体，以及所公开的化合物和组合物在治疗通过施用去头痛肾上腺素/ 5-羟色胺再摄取抑制剂（NSRI）有益治疗的疾病和病症的方法中的用途，，这样我们milnacipran。

9. 发明申请

WO2010005520A3 DEUTERATED IBUDILAST 审中-公开
公开(公告)号：WO2010005520A3
公开(公告)日：2010-03-04
申请号：PCT/US2009003888
申请日：2009-06-30
申请人： CONCERT PHARMACEUTICALS INC , LIU JULIE F , PERSICHETTI ROSE A
发明人： LIU JULIE F , PERSICHETTI ROSE A
IPC分类号： C07D471/04 , A61K31/437 , A61P11/06
CPC分类号： C07D471/04
摘要： This invention relates to novel compounds that are 2-alkyl-3-acylpyrazolo[l,5- a]pyridines, their derivatives, and pharmaceutically acceptable salts thereof. More specifically, the invention relates to 2-alkyl-3-acylpyrazolo[l,5-a]pyridine compounds that are derivatives of ibudilast. This invention also provides compositions comprising a compound of this invention and the use of such compositions in methods of treating diseases and conditions that are beneficially treated by administering a phosphodiesterase (PDE) inhibitor, a leukotriene CysLTl (LTD4) antagonist, an inhibitor of nitric oxide synthase, and/or a glial cell activation suppressant, such as ibudilast.
摘要翻译：本发明涉及2-烷基-3-酰基吡唑并[1,5-a]吡啶，其衍生物及其药学上可接受的盐的新化合物。更具体地，本发明涉及作为异丁司特衍生物的2-烷基-3-酰基吡唑并[1,5-a]吡啶化合物。本发明还提供包含本发明化合物和这些组合物在治疗通过施用磷酸二酯酶（PDE）抑制剂，白三烯CysLT1（LTD4）拮抗剂，一氧化氮抑制剂）有益治疗的疾病和病症的方法中的用途合成酶和/或神经胶质细胞活化抑制剂，例如异丁司特。

10. 发明申请

WO2010019560A1 DEUTERATED DERIVATIVES OF DONEPEZIL 审中-公开
标题翻译：二苯醚的去除衍生物
公开(公告)号：WO2010019560A1
公开(公告)日：2010-02-18
申请号：PCT/US2009/053390
申请日：2009-08-11
申请人： CONCERT PHARMACEUTICALS INC. , LIU, Julie, F.
发明人： LIU, Julie, F.
IPC分类号： C07D211/32 , C07B59/00 , A61K31/445 , A61P25/28
CPC分类号： C07D211/32 , C07B59/002
摘要： This invention relates to deuterated derivatives of donezepil and its metabolites as well as pharmaceutically acceptable salts thereof. This invention also provides compositions comprising a compound of this invention and the use of such compositions in methods of treating diseases and conditions that are beneficially treated by administering acetylcholinesterase inhibitors.
摘要翻译：本发明涉及替扎平及其代谢产物的氘代衍生物及其药学上可接受的盐。本发明还提供了包含本发明化合物的组合物和这些组合物在治疗通过施用乙酰胆碱酯酶抑制剂有益治疗的疾病和病症的方法中的用途。

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