公开(公告)号：EP3154966B1

公开(公告)日：2019-05-08

申请号：EP15730666.3

申请日：2015-06-12

申请人： The U.S.A. as represented by the Secretary, Department of Health and Human Services ,  University of Kansas

发明人： LIANG,Tsanyang ,  HU, Zongyi ,  MARUGAN, Juan Jose ,  SOUTHALL, Noel Terrence ,  HE, Shanshan ,  HU, Xin ,  XIAO, Jingbo ,  FERRER, Marc ,  ZHENG, Wei ,  FRANKOWSKI, Kevin J. ,  SCHOENEN, Frank J. ,  LI, Kelin

IPC分类号： C07D413/14 ,  C07D471/08 ,  A61K31/553 ,  A61P31/14

公开(公告)号：EP3154966A1

公开(公告)日：2017-04-19

申请号：EP15730666.3

申请日：2015-06-12

申请人： The U.S.A. as represented by the Secretary, Department of Health and Human Services ,  University of Kansas

发明人： LIANG,Tsanyang ,  HU, Zongyi ,  MARUGAN, Juan Jose ,  SOUTHALL, Noel Terrence ,  HE, Shanshan ,  HU, Xin ,  XIAO, Jingbo ,  FERRER, Marc ,  ZHENG, Wei ,  FRANKOWSKI, Kevin J. ,  SCHOENEN, Frank J. ,  LI, Kelin

IPC分类号： C07D413/14 ,  C07D471/08 ,  A61K31/553 ,  A61P31/14

CPC分类号： C07D413/06 ,  A61K31/4178 ,  A61K31/454 ,  A61K31/4545 ,  A61K31/496 ,  A61K31/5377 ,  A61K31/7056 ,  A61K31/7068 ,  A61K38/07 ,  A61K38/13 ,  A61K38/212 ,  C07D413/14 ,  C07D417/14 ,  C07D471/08 ,  Y02A50/385

摘要： Disclosed are compounds of formula (I), formula (II), and formula (III): wherein Ar, R1, A, and X are as defined in the specification. These compounds are antiviral agents and are contemplated for use in the treatment of viral infections, for example, hepatitis C. These compounds are also contemplated for use in treating or preventing cancers.

摘要翻译： 公开了式（I），式（II）和式（III）的化合物：其中Ar，R 1，A和X如说明书中所定义。 这些化合物是抗病毒剂，并且被考虑用于治疗病毒感染，例如丙型肝炎。这些化合物也被考虑用于治疗或预防癌症。

公开(公告)号：EP2595623A1

公开(公告)日：2013-05-29

申请号：EP11741023.3

申请日：2011-07-19

申请人： The U.S.A. as represented by the Secretary, Department of Health and Human Services

发明人： ZHENG, Wei ,  MARUGAN, Juan Jose ,  LIU, Ke ,  SOUTHALL, Noel Terrence ,  AUSTIN, Christopher P.

IPC分类号： A61K31/355 ,  A61P43/00

CPC分类号： A61K31/355 ,  A61K31/36 ,  A61K31/496 ,  A61K31/724 ,  A61K36/185 ,  A61K45/06 ,  A61K2300/00

摘要： This disclosure relates generally to the treatment of lysosomal storage disorders. Specifically, the disclosure relates to a novel use of delta tocopherol in the treatment of diseases and conditions related to lysosomal storage disorders. Included in the present disclosure is a method for the modulation of cholesterol recycling. Further, the disclosure relates to conditions such as Niemann-Pick type C disease, Farber disease, Niemann-Pick type A disease, Wolman disease and Tay Sachs disease. Further included in the present disclosure is a method for treating lysosomal storage disorders comprising the administration of delta tocopherol. Further included in the present disclosure is a method for treating lysosomal storage disorders comprising the administration of delta tocopherol in combination with cyclodextrin to a patient in need thereof.

摘要翻译： 本公开一般涉及溶酶体储存障碍的治疗。 具体地，本公开涉及δ生育酚在治疗与溶酶体贮积障碍有关的疾病和病症中的新用途。 包括在本公开内容中的是调节胆固醇回收的方法。 此外，本公开涉及诸如Niemann-Pick型C型疾病，Farber病，Niemann-Pick型A型疾病，Wolman病和Tay Sachs病等病症。 本公开内容中还包括用于治疗溶酶体储存障碍的方法，其包括施用δ-生育酚。 本公开内容中还包括用于治疗溶酶体贮积症的方法，其包括与需要的患者一起向环糊精施用δ-生育酚。

公开(公告)号：EP3027612B1

公开(公告)日：2018-10-10

申请号：EP14750663.8

申请日：2014-07-29

申请人： The U.S.A. as represented by the Secretary, Department of Health and Human Services

发明人： MARUGAN, Juan Jose ,  XIAO, Jingbo ,  FERRER, Marc ,  SOUTHALL, Noel Terrence ,  FREE, R. Benjamin ,  SIBLEY, David Robert

IPC分类号： C07D417/12 ,  C07D281/16 ,  A61K31/554 ,  A61P25/14 ,  A61P25/18 ,  A61P25/24

CPC分类号： C07D281/16 ,  C07D417/12

摘要： The disclosure includes compounds and pharmaceutically acceptable salts of Formula (I). Certain compounds and salts of Formula (I) are selective inhibitors of the Dopamine D2 receptor. The variables R1-R4, n, and L are defined herein. The disclosure also provides methods of synthesizing compounds of Formula (I) and pharmaceutical compositions containing compounds of Formula (I). Additionally the disclosure provides methods or treating patients suffering from central nervous system disorders, including Tourette's syndrome, bipolar disorder, hyperprolactinemia, tardive dyskinesia, Huntington's chorea, psychosis, depression, or schizophrenia.

公开(公告)号：EP2595623B1

公开(公告)日：2018-02-28

申请号：EP11741023.3

申请日：2011-07-19

申请人： The U.S.A. as represented by the Secretary, Department of Health and Human Services

发明人： ZHENG, Wei ,  MARUGAN, Juan Jose ,  LIU, Ke ,  SOUTHALL, Noel Terrence ,  AUSTIN, Christopher P.

IPC分类号： A61K31/355 ,  A61P43/00

CPC分类号： A61K31/355 ,  A61K31/36 ,  A61K31/496 ,  A61K31/724 ,  A61K36/185 ,  A61K45/06 ,  A61K2300/00

摘要： This disclosure relates generally to the treatment of lysosomal storage disorders. Specifically, the disclosure relates to a novel use of delta tocopherol in the treatment of diseases and conditions related to lysosomal storage disorders. Included in the present disclosure is a method for the modulation of cholesterol recycling. Further, the disclosure relates to conditions such as Niemann-Pick type C disease, Farber disease, Niemann-Pick type A disease, Wolman disease and Tay Sachs disease. Further included in the present disclosure is a method for treating lysosomal storage disorders comprising the administration of delta tocopherol. Further included in the present disclosure is a method for treating lysosomal storage disorders comprising the administration of delta tocopherol in combination with cyclodextrin to a patient in need thereof.

公开(公告)号：EP3074001A1

公开(公告)日：2016-10-05

申请号：EP14809235.6

申请日：2014-11-20

申请人： The U.S.A. as represented by the Secretary, Department of Health and Human Services

发明人： LIANG, Tsanyang Jake ,  FERRER, Marc ,  HE, Shanshan ,  HU, Xin ,  HU, Zongyi ,  MARUGAN, Juan Jose ,  SOUTHALL, Noel Terrence ,  XIAO, Jingbo ,  ZHENG, Wei

IPC分类号： A61K31/12 ,  A61K35/00 ,  A61K31/4468 ,  A61K31/4465 ,  A61K31/445 ,  A61K31/4995 ,  C07D243/08 ,  C07D295/073 ,  C07D295/088 ,  C07D295/096 ,  C07D295/185 ,  C07D209/48 ,  A61P31/12 ,  A61P35/00

CPC分类号： C07D405/10 ,  A61K31/4409 ,  A61K31/4465 ,  A61K31/4468 ,  A61K31/453 ,  A61K31/495 ,  A61K31/496 ,  A61K31/55 ,  A61K45/06 ,  C07D209/48 ,  C07D211/12 ,  C07D211/14 ,  C07D211/58 ,  C07D213/16 ,  C07D243/08 ,  C07D295/03 ,  C07D295/073 ,  C07D295/088 ,  C07D295/096 ,  C07D295/185 ,  C07D403/12

摘要： Disclosed are compounds of formula (I) (formula I),as antiviral agents, antineoplastic agents, pharmaceutical compositions comprising such compounds, and a method of use of these compounds, wherein X and Y are independently CH or N, o is 0, 1 or 2, and E is absent or is (CR
13 R
14 )m, NH, or S, F is absent or is (CR
15 R
16 )n, C=O, or -SO
2 -, G is absent or is (CR
17 CR
18 )r, H is absent or is C=O, or -SO
2 - and R
1 , Ar
1 , Ar
2 are as defined in the specification. These compounds are antiviral agents and are contemplated in the treatment of viral infections, for example, hepatitis C, or are antineoplastic agents.

摘要翻译： 本发明公开了式（I）（式I），作为抗病毒剂，抗肿瘤剂，药物组合物，包含检查化合物，和使用合成的化合物的方法，worin X和Y独立地是CH或N，o为0，1的化合物 或2，e是不存在或（CR 13 R 14）米，NH或S，R不存在或为（CR 15 R 16）N，C = O，或-SO 2 - ，G是不存在或为（CR17 CR18）R H是不存在或为C = O，-SO 2或 - 且R 1中，Ar 1中，Ar 2是如说明书中所定义。 这些化合物的抗病毒剂和病毒感染的治疗被预期，例如，丙型肝炎，或是抗肿瘤剂。

公开(公告)号：EP3027612A1

公开(公告)日：2016-06-08

申请号：EP14750663.8

申请日：2014-07-29

申请人： The U.S.A. as represented by the Secretary, Department of Health and Human Services

发明人： MARUGAN, Juan Jose ,  XIAO, Jingbo ,  FERRER, Marc ,  SOUTHALL, Noel Terrence ,  FREE, R. Benjamin ,  SIBLEY, David Robert

IPC分类号： C07D417/12 ,  C07D281/16 ,  A61K31/554 ,  A61P25/14 ,  A61P25/18 ,  A61P25/24

CPC分类号： C07D281/16 ,  C07D417/12

摘要： The disclosure includes compounds and pharmaceutically acceptable salts of Formula (I). Certain compounds and salts of Formula (I) are selective inhibitors of the Dopamine D2 receptor. The variables R1-R4, n, and L are defined herein. The disclosure also provides methods of synthesizing compounds of Formula (I) and pharmaceutical compositions containing compounds of Formula (I). Additionally the disclosure provides methods or treating patients suffering from central nervous system disorders, including Tourette's syndrome, bipolar disorder, hyperprolactinemia, tardive dyskinesia, Huntington's chorea, psychosis, depression, or schizophrenia.

摘要翻译： 本公开内容包括式（I）的化合物和药学上可接受的盐。 某些化合物和式（I）的盐是多巴胺D2受体的选择性抑制剂。 变量R1-R4，n和L在本文中定义。 本公开还提供了合成式（I）化合物和含有式（I）化合物的药物组合物的方法。 此外，本公开提供了方法或治疗患有中枢神经系统疾病的患者，包括图雷特综合征，双相情感障碍，高催乳素血症，迟发性运动障碍，亨廷顿舞蹈病，精神病，抑郁症或精神分裂症。

公开(公告)号：EP3442955A1

公开(公告)日：2019-02-20

申请号：EP17733098.2

申请日：2017-04-14

申请人： The United States Of America, As Represented By The Secretary, Department Of Health And Human Services ,  The University of Kansas

发明人： SIBLEY, David R. ,  MORITZ, Amy Elizabeth ,  FREE, R. Benjamin ,  STEINER, Joseph P. ,  SOUTHALL, Noel Terrence ,  FERRER, Marc ,  HU, Xin ,  WEINER, Warren S. ,  AUBÉ, Jeffrey ,  FRANKOWSKI, Kevin

IPC分类号： C07D333/70 ,  C07D339/06 ,  C07D401/12 ,  C07D235/24 ,  C07D405/12 ,  C07D409/12 ,  C07D471/04 ,  C07D209/42 ,  C07D295/192 ,  C07D307/85 ,  A61P25/16 ,  A61P25/28 ,  A61P25/14