公开(公告)号：US09452973B2

公开(公告)日：2016-09-27

申请号：US14398830

申请日：2013-03-15

申请人： The United States of America, as Represented by the Secretary, Department of Health and Human Service ,  The Florida International University Board of Trustees

发明人： Juan Jose Marugan ,  Jingbo Xiao ,  Marc Ferrer-Alegre ,  Catherine Chen ,  Noel Southall ,  Wei Zheng ,  Alexander Agoulnik ,  Irina Agoulnik

IPC分类号： A61K31/166 ,  C07C233/64 ,  C07C237/42 ,  C07C255/57 ,  C07D213/75 ,  C07C255/60 ,  C07C257/18 ,  C07D213/79 ,  C07D213/80 ,  C07D213/81 ,  C07D213/82 ,  C07C271/28 ,  C07D317/68 ,  C07D333/20 ,  C07D333/38 ,  C07D333/40 ,  C07C311/29 ,  C07D235/18 ,  C07C323/62 ,  C07C257/04 ,  C07C233/63 ,  C07D261/18 ,  C07C235/64 ,  C07C237/30 ,  C07C237/40 ,  C07D209/08 ,  C07D209/46 ,  C07D295/088 ,  C07D295/205 ,  C07D307/52 ,  C07D307/68 ,  C07D317/66 ,  C07D235/06 ,  C07D403/10 ,  C07D487/04 ,  C07D295/135 ,  C07C317/36 ,  C07C317/40 ,  C07C317/44 ,  C07C323/42

CPC分类号： C07D333/38 ,  C07C233/63 ,  C07C235/64 ,  C07C237/30 ,  C07C237/40 ,  C07C237/42 ,  C07C251/24 ,  C07C255/57 ,  C07C255/60 ,  C07C257/04 ,  C07C257/18 ,  C07C271/28 ,  C07C311/29 ,  C07C317/36 ,  C07C317/40 ,  C07C317/44 ,  C07C323/42 ,  C07C323/62 ,  C07C2601/02 ,  C07C2601/04 ,  C07C2601/10 ,  C07C2601/14 ,  C07C2601/16 ,  C07C2601/18 ,  C07C2602/08 ,  C07C2603/74 ,  C07D209/08 ,  C07D209/46 ,  C07D211/26 ,  C07D213/75 ,  C07D213/79 ,  C07D213/80 ,  C07D213/81 ,  C07D213/82 ,  C07D235/06 ,  C07D235/08 ,  C07D235/14 ,  C07D235/18 ,  C07D257/04 ,  C07D261/18 ,  C07D295/088 ,  C07D295/135 ,  C07D295/205 ,  C07D307/52 ,  C07D307/68 ,  C07D317/66 ,  C07D317/68 ,  C07D333/20 ,  C07D333/40 ,  C07D403/10 ,  C07D487/04

摘要： Disclosed are modulators of the human relaxin receptor 1, for example, of formula (I), wherein A, R1, and R2 are as defined herein, that are useful in treating mammalian relaxin receptor 1 mediated facets of human health, e.g., cardiovascular disease. Also disclosed is a composition comprising a pharmaceutically suitable carrier and at least one compound of the disclosure, and a method for therapeutic intervention in a facet of mammalian health that is mediated by a human relaxin receptor 1.

摘要翻译： 公开了人类松弛素受体1的调节剂，例如式（I）的化合物，其中A，R 1和R 2如本文所定义，其可用于治疗哺乳动物松弛素受体1介导的人体健康方面，例如心血管疾病 。 还公开了包含药学上合适的载体和本公开的至少一种化合物的组合物，以及由人松弛素受体1介导的哺乳动物健康的方面的治疗性干预的方法。

公开(公告)号：US10125112B2

公开(公告)日：2018-11-13

申请号：US15247438

申请日：2016-08-25

申请人： The United States of America, as Represented by the Secretary, Department of Health and Human Service ,  The Florida International University Board of Trustees

发明人： Juan Jose Marugan ,  Jingbo Xiao ,  Marc Ferrer-Alegre ,  Catherine Chen ,  Noel Southall ,  Wei Zheng ,  Alexander Agoulnik ,  Irina Agoulnik

IPC分类号： C07C233/64 ,  A61K31/166 ,  C07D333/38 ,  C07C237/42 ,  C07D307/52 ,  C07D333/20 ,  C07D317/68 ,  C07D213/81 ,  C07D307/68 ,  C07D213/82 ,  C07D261/18 ,  C07D209/08 ,  C07D317/66 ,  C07C317/40 ,  C07C323/42 ,  C07D211/26 ,  C07D295/088 ,  C07D235/08 ,  C07D295/205 ,  C07D235/14 ,  C07C255/60 ,  C07D257/04 ,  C07C251/24

摘要： Disclosed are modulators of the human relaxin receptor 1, for example, of formula (I), wherein A, R1, and R2 are as defined herein, that are useful in treating mammalian relaxin receptor 1 mediated facets of human health, e.g., cardiovascular disease. Also disclosed is a composition comprising a pharmaceutically suitable carrier and at least one compound of the disclosure, and a method for therapeutic intervention in a facet of mammalian health that is mediated by a human relaxin receptor 1.

公开(公告)号：US10925874B2

公开(公告)日：2021-02-23

申请号：US15983844

申请日：2018-05-18

申请人： The United States of America, as Represented by the Secretary, Department of Health and Human Service

发明人： Juan Jose Marugan ,  Noel Southall ,  Ehud Goldin ,  Wei Zheng ,  Samarjit Patnaik ,  Ellen Sidransky ,  Omid Motabar ,  Wendy Westbroek

IPC分类号： C07D487/02 ,  A61K31/519 ,  A61P43/00 ,  C07D487/04 ,  A61K31/5377

摘要： Substituted pyrazolopyrimidines and dihydropyrazolopyrimidines and related compounds, their methods of manufacture, compositions containing these compounds, and methods of use of these compounds in treating lysosomal storage disorders such as Gaucher disease are described herein. The compounds are of general Formula (I) in which variables R1-R7 and X are described in the application.

公开(公告)号：US20140323438A1

公开(公告)日：2014-10-30

申请号：US14364759

申请日：2012-12-17

申请人： The United States of America,as represented by the Secretary, Department of Health and Human Service

发明人： Kevin Frankowski ,  Samarjit Patnaik ,  Sui Huang ,  Juan Jose Marugan ,  John Norton ,  Frank J. Schoenen ,  Noel Terrence Southall ,  Steven Titus ,  Wei Zheng

IPC分类号： C07D487/04 ,  C07F7/18 ,  A61K45/06 ,  A61K31/695 ,  A61K31/519

CPC分类号： C07D487/04 ,  A61K31/519 ,  A61K31/695 ,  A61K45/06 ,  C07F7/1804

摘要： The disclosure provides compounds for reducing the prevalence of the perinucleolar compartment in cells, for example, of formula (I), wherein R1, R2, R3, and R4 are as defined herein, that are useful in treating a disease or disorder associated with increased prevalence of the perinucleolar compartment, such as cancer. Also disclosed is a composition containing a pharmaceutically acceptable carrier and at least one compound embodying the principles of the invention, and a method of treating or preventing cancer in a mammal.

摘要翻译： 本公开内容提供了用于降低细胞中例如式（I）的细胞周围隔室的化合物，其中R 1，R 2，R 3和R 4如本文所定义，其可用于治疗与增加的疾病或病症相关的疾病或病症 周围隔室的流行，如癌症。 还公开了含有药学上可接受的载体和至少一种体现本发明原理的化合物以及治疗或预防哺乳动物癌症的方法的组合物。

公开(公告)号：US20170144984A1

公开(公告)日：2017-05-25

申请号：US15247438

申请日：2016-08-25

申请人： The United States of America, as Represented by Secretary, Department of Health and Human Service ,  The Florida International University Board of Trustees

发明人： Juan Jose Marugan ,  Jingbo Xiao ,  Marc Ferrer-Alegre ,  Catherine Chen ,  Noel Southall ,  Wei Zheng ,  Alexander Agoulnik ,  Irina Agoulnik

IPC分类号： C07D333/38 ,  C07D307/52 ,  C07D333/20 ,  C07D317/68 ,  C07D213/81 ,  C07D307/68 ,  C07D213/82 ,  C07D261/18 ,  C07D209/08 ,  C07D317/66 ,  C07C317/40 ,  C07C323/42 ,  C07D211/26 ,  C07D295/088 ,  C07D235/08 ,  C07D295/205 ,  C07D235/14 ,  C07C255/60 ,  C07D257/04 ,  C07C251/24 ,  C07C237/42

CPC分类号： C07D333/38 ,  C07C233/63 ,  C07C235/64 ,  C07C237/30 ,  C07C237/40 ,  C07C237/42 ,  C07C251/24 ,  C07C255/57 ,  C07C255/60 ,  C07C257/04 ,  C07C257/18 ,  C07C271/28 ,  C07C311/29 ,  C07C317/36 ,  C07C317/40 ,  C07C317/44 ,  C07C323/42 ,  C07C323/62 ,  C07C2601/02 ,  C07C2601/04 ,  C07C2601/10 ,  C07C2601/14 ,  C07C2601/16 ,  C07C2601/18 ,  C07C2602/08 ,  C07C2603/74 ,  C07D209/08 ,  C07D209/46 ,  C07D211/26 ,  C07D213/75 ,  C07D213/79 ,  C07D213/80 ,  C07D213/81 ,  C07D213/82 ,  C07D235/06 ,  C07D235/08 ,  C07D235/14 ,  C07D235/18 ,  C07D257/04 ,  C07D261/18 ,  C07D295/088 ,  C07D295/135 ,  C07D295/205 ,  C07D307/52 ,  C07D307/68 ,  C07D317/66 ,  C07D317/68 ,  C07D333/20 ,  C07D333/40 ,  C07D403/10 ,  C07D487/04

摘要： Disclosed are modulators of the human relaxin receptor 1, for example, of formula (I), wherein A, R1, and R2 are as defined herein, that are useful in treating mammalian relaxin receptor 1 mediated facets of human health, e.g., cardiovascular disease. Also disclosed is a composition comprising a pharmaceutically suitable carrier and at least one compound of the disclosure, and a method for therapeutic intervention in a facet of mammalian health that is mediated by a human relaxin receptor 1.

公开(公告)号：US20150119426A1

公开(公告)日：2015-04-30

申请号：US14398830

申请日：2013-03-15

申请人： The United States of America, as Represented by the Secretary, Dept. of Health & Human Services ,  The Florida International University Board of Trustees

发明人： Juan Jose Marugan ,  Jingbo Xiao ,  Marc Ferrer-Alegre ,  Catherine Chen ,  Noel Southall ,  Wei Zheng ,  Alexander Agoulnik ,  Irina Agoulnik

IPC分类号： C07C237/42 ,  C07D213/81 ,  C07D333/38 ,  C07D213/82 ,  C07C323/42 ,  C07C317/40

CPC分类号： C07D333/38 ,  C07C233/63 ,  C07C235/64 ,  C07C237/30 ,  C07C237/40 ,  C07C237/42 ,  C07C251/24 ,  C07C255/57 ,  C07C255/60 ,  C07C257/04 ,  C07C257/18 ,  C07C271/28 ,  C07C311/29 ,  C07C317/36 ,  C07C317/40 ,  C07C317/44 ,  C07C323/42 ,  C07C323/62 ,  C07C2601/02 ,  C07C2601/04 ,  C07C2601/10 ,  C07C2601/14 ,  C07C2601/16 ,  C07C2601/18 ,  C07C2602/08 ,  C07C2603/74 ,  C07D209/08 ,  C07D209/46 ,  C07D211/26 ,  C07D213/75 ,  C07D213/79 ,  C07D213/80 ,  C07D213/81 ,  C07D213/82 ,  C07D235/06 ,  C07D235/08 ,  C07D235/14 ,  C07D235/18 ,  C07D257/04 ,  C07D261/18 ,  C07D295/088 ,  C07D295/135 ,  C07D295/205 ,  C07D307/52 ,  C07D307/68 ,  C07D317/66 ,  C07D317/68 ,  C07D333/20 ,  C07D333/40 ,  C07D403/10 ,  C07D487/04

摘要： Disclosed are modulators of the human relaxin receptor 1, for example, of formula (I), wherein A, R1, and R2 are as defined herein, that are useful in treating mammalian relaxin receptor 1 mediated facets of human health, e.g., cardiovascular disease. Also disclosed is a composition comprising a pharmaceutically suitable carrier and at least one compound of the disclosure, and a method for therapeutic intervention in a facet of mammalian health that is mediated by a human relaxin receptor 1.

摘要翻译： 公开了人类松弛素受体1的调节剂，例如式（I）的化合物，其中A，R 1和R 2如本文所定义，其可用于治疗哺乳动物松弛素受体1介导的人体健康方面，例如心血管疾病 。 还公开了包含药学上合适的载体和本公开的至少一种化合物的组合物，以及由人松弛素受体1介导的哺乳动物健康的方面的治疗性干预的方法。