公开(公告)号：WO2010051031A1

公开(公告)日：2010-05-06

申请号：PCT/US2009/005898

申请日：2009-10-30

Applicant: BIOGEN IDEC MA INC. ,  GUCKIAN, Kevin, M. ,  CALDWELL, Richard, D. ,  KUMARAVEL, Gnanasambandam ,  LEE, Wen-cherng ,  LIN, Edward, Yin-shiang ,  LIU, Xiaogao ,  MA, Bin ,  SCOTT, Daniel, M. ,  SHI, Zhan ,  ZHENG, Guo, Zhu ,  TAVERAS, Arthur, G. ,  THOMAS, Jermaine

Inventor： GUCKIAN, Kevin, M. ,  CALDWELL, Richard, D. ,  KUMARAVEL, Gnanasambandam ,  LEE, Wen-cherng ,  LIN, Edward, Yin-shiang ,  LIU, Xiaogao ,  MA, Bin ,  SCOTT, Daniel, M. ,  SHI, Zhan ,  ZHENG, Guo, Zhu ,  TAVERAS, Arthur, G. ,  THOMAS, Jermaine

IPC: A01N47/10 ,  A61K31/22 ,  A61K31/135

CPC classification number: A61K31/135 ,  A61K31/22 ,  C07C217/52 ,  C07C217/74 ,  C07C2602/10 ,  C07D215/20 ,  C07D239/74

Abstract: Compounds that have agonist activity at one or more of the SlP receptors are provided. The compounds are sphingosine analogs that, after phosphorylation, can behave as agonists at SlP receptors.

Abstract translation: 提供了在一种或多种S1P受体上具有激动剂活性的化合物。 化合物是鞘氨醇类似物，其在磷酸化之后可以作为S1P受体的激动剂。

公开(公告)号：WO2005016890A1

公开(公告)日：2005-02-24

申请号：PCT/US2004/025109

申请日：2004-08-04

Applicant: ABBOTT LABORATORIES ,  LEE, Chih-Hung ,  BAYBURT, Erol, K. ,  DIDOMENICO, Stanley, Jr. ,  DRIZIN, Irene ,  GOMTSYAN, Arthur, R. ,  KOENIG, John, R. ,  PENNER, Richard, J. ,  SCHMIDT, Robert, G., Jr. ,  TURNER, Sean, C. ,  WHITE, Tammie, K. ,  ZHENG, Guo Zhu

Inventor： BAYBURT, Erol, K. ,  DIDOMENICO, Stanley, Jr. ,  DRIZIN, Irene ,  GOMTSYAN, Arthur, R. ,  KOENIG, John, R. ,  PENNER, Richard, J. ,  SCHMIDT, Robert, G., Jr. ,  TURNER, Sean, C. ,  WHITE, Tammie, K. ,  ZHENG, Guo Zhu

IPC: C07D217/24

CPC classification number: C07D249/08 ,  C07D209/08 ,  C07D217/02 ,  C07D217/22 ,  C07D217/24 ,  C07D217/26 ,  C07D231/12 ,  C07D231/56 ,  C07D233/56 ,  C07D237/28 ,  C07D401/12 ,  C07D405/12

Abstract: Compounds of Formula (I), are novel VR1 antagonists that are useful in treating pain, inflammatory thermal hyperalgesia, urinary incontinence and bladder overactivity.

Abstract translation: 式（I）化合物是可用于治疗疼痛，炎症性热痛觉过敏，尿失禁和膀胱过度活动的新型VR1拮抗剂。

公开(公告)号：WO2018098305A1

公开(公告)日：2018-05-31

申请号：PCT/US2017/063047

申请日：2017-11-22

Applicant: EISAI R&D MANAGEMENT CO., LTD. ,  BOCK, Mark ,  HAO, Ming-Hong ,  KORPAL, Manav ,  NYAVANANDI, Vijay Kumar ,  PUYANG, Xiaoling ,  SAMAJDAR, Susanta ,  SMITH, Peter Gerard ,  WANG, John ,  ZHENG, Guo Zhu ,  ZHU, Ping ,  MITCHELL, Lorna Helen ,  LARSEN, Nicholas ,  RIOUX, Nathalie ,  PRAJAPATI, Sudeep ,  REYNOLDS, Dominic ,  O'SHEA, Morgan ,  SAMARAKOON, Thiwanka

Inventor： BOCK, Mark ,  HAO, Ming-Hong ,  KORPAL, Manav ,  NYAVANANDI, Vijay Kumar ,  PUYANG, Xiaoling ,  SAMAJDAR, Susanta ,  SMITH, Peter Gerard ,  WANG, John ,  ZHENG, Guo Zhu ,  ZHU, Ping ,  MITCHELL, Lorna Helen ,  LARSEN, Nicholas ,  RIOUX, Nathalie ,  PRAJAPATI, Sudeep ,  REYNOLDS, Dominic ,  O'SHEA, Morgan ,  SAMARAKOON, Thiwanka

IPC: C07D403/12 ,  C07D401/14 ,  C07D231/56 ,  C07D401/06 ,  A61P35/00 ,  A61K31/416

Abstract: Disclosed herein are compounds, or pharmaceutically acceptable salts thereof, and methods of using the compounds for treating breast cancer by administration to a subject in need thereof a therapeutically effective amount of the compounds or pharmaceutically acceptable salts thereof. The breast cancer may be an ER-positive breast cancer and/or the subject in need of treatment may express a mutant ER-α protein.

公开(公告)号：WO2018098251A1

公开(公告)日：2018-05-31

申请号：PCT/US2017/062978

申请日：2017-11-22

Applicant: EISAI R&D MANAGEMENT CO., LTD. ,  BOCK, Mark ,  HAO, Ming-Hong ,  KORPAL, Manav ,  NYAVANANDI, Vijay Kumar ,  PUYANG, Xiaoling ,  SAMAJDAR, Susanta ,  SMITH, Peter Gerard ,  WANG, John ,  ZHENG, Guo Zhu ,  ZHU, Ping ,  MITCHELL, Lorna Helen ,  LARSEN, Nicholas ,  RIOUX, Nathalie

Inventor： BOCK, Mark ,  HAO, Ming-Hong ,  KORPAL, Manav ,  NYAVANANDI, Vijay Kumar ,  PUYANG, Xiaoling ,  SAMAJDAR, Susanta ,  SMITH, Peter Gerard ,  WANG, John ,  ZHENG, Guo Zhu ,  ZHU, Ping ,  MITCHELL, Lorna Helen ,  LARSEN, Nicholas ,  RIOUX, Nathalie

IPC: C07D209/08 ,  A61P35/00

Abstract: Disclosed herein are compounds, or pharmaceutically acceptable salts thereof, and methods of using the compounds for treating breast cancer by administration to a subject in need thereof a therapeutically effective amount of the compounds or pharmaceutically acceptable salts thereof. The breast cancer may be an ER-positive breast cancer and/or the subject in need of treatment may express a mutant ER-α protein.

公开(公告)号：WO2017087667A1

公开(公告)日：2017-05-26

申请号：PCT/US2016/062525

申请日：2016-11-17

Applicant: EISAI R&D MANAGEMENT CO., LTD. ,  KEANEY, Gregg F. ,  WANG, John ,  GERARD, Baudouin ,  ARAI, Kenzo ,  LIU, Xiang ,  ZHENG, Guo, Zhu ,  KIRA, Kazunobu ,  TIVITMAHAISOON, Parcharee ,  PRAJAPATI, Sudeep ,  GEARHART, Nicholas C. ,  KOTAKE, Yoshihiko ,  NAGAO, Satoshi ,  KANADA SONABE, Regina, Mikie ,  MIYANO, Masayuki ,  MURAI, Norio ,  BUONAMICI, Silvia ,  YU, Lihua ,  PARK, Eunice, Sun ,  CHAN, Betty ,  SMITH, Peter, G. ,  THOMAS, Michael P. ,  PAZOLLI, Ermira ,  LIM, Kian, Huat

Inventor： KEANEY, Gregg F. ,  WANG, John ,  GERARD, Baudouin ,  ARAI, Kenzo ,  LIU, Xiang ,  ZHENG, Guo, Zhu ,  KIRA, Kazunobu ,  TIVITMAHAISOON, Parcharee ,  PRAJAPATI, Sudeep ,  KOTAKE, Yoshihiko ,  KANADA SONABE, Regina, Mikie ,  MIYANO, Masayuki ,  MURAI, Norio ,  BUONAMICI, Silvia ,  YU, Lihua ,  PARK, Eunice, Sun ,  SMITH, Peter, G. ,  PAZOLLI, Ermira ,  LIM, Kian, Huat

IPC: C07D405/06 ,  A61K31/4427 ,  A61P35/00

CPC classification number: C07D405/06

Abstract: The present disclosure provides a novel solid state form of pladienolide pyridine compounds, compositions comprising at least one such solid state form, and methods of preparation and use and the same. The novel solid state form of pladienolide pyridine compounds may be useful in the treatment of cancer, such as, for example, cancers in which agents that target the spliceosome and mutations therein are known to be useful.

Abstract translation: 本公开提供了一种新型固体形式的普拉二烯内酯吡啶化合物，包含至少一种此类固体形式的组合物，以及制备和使用方法及其相关方法。 该新型固体形式的普拉二烯内酯吡啶化合物可用于治疗癌症，例如癌症，其中靶向剪接体的试剂及其突变已知是有用的。

公开(公告)号：WO2007100990A3

公开(公告)日：2007-09-07

申请号：PCT/US2007/062329

申请日：2007-02-16

Applicant: ABBOTT LABORATORIES ,  COWART, Marlon, D. ,  ZHAO, Chen ,  SUN, Minghua ,  BLACK, Lawrence, A. ,  ZHENG, Guo Zhu ,  GREGG, Robert, J. ,  ZHANG, Geoff, G.Z. ,  SHEIKH, Ahmad, Y. ,  LOU, Xiaochun ,  HENRY, Rodger, F. ,  BARNES, David, M. ,  KOLACZKOWSKI, Lawrence ,  HAIGHT, Anthony, R. ,  CHANG, Sou-Jen ,  WITTENBERGER, Steven, J. ,  FICKES, Michael, G.

Inventor： COWART, Marlon, D. ,  ZHAO, Chen ,  SUN, Minghua ,  BLACK, Lawrence, A. ,  ZHENG, Guo Zhu ,  GREGG, Robert, J. ,  ZHANG, Geoff, G.Z. ,  SHEIKH, Ahmad, Y. ,  LOU, Xiaochun ,  HENRY, Rodger, F. ,  BARNES, David, M. ,  KOLACZKOWSKI, Lawrence ,  HAIGHT, Anthony, R. ,  CHANG, Sou-Jen ,  WITTENBERGER, Steven, J. ,  FICKES, Michael, G.

IPC: C07D487/04 ,  A61K31/407

Abstract: Octahydro-pyrrolo[3,4-b]pyrrole derivatives or a pharmaceutically acceptable salt, ester, amide, prodrug, or radiolabeled form thereof, wherein R 1 is alkyl, C 3 -C 5 cycloalkyl. or (C 3 -C 5 cycloalkyl)methyl; R 2a , R 2b , R 2c , R 2d , R 2e , and R 2f each are independently hydrogen, methyl, or fluoromethyl; R 3a , R 3b , R 3c , and R 3d each are independently hydrogen, alkyl, fluoroalkyl, fluoroalkoxy, alkoxy, thioalkoxy, halogen, or nitrile, with the proviso that when one or more of R 3a , R 3b , R 3c , and R 3d are alkyl, then at least one of R 3a , R 3b , R 3c , and R 3d is fluoroalkyl, fluoroalkoxy, alkoxy, thioalkoxy, halogen, or nitrile; L 1 is a bond, oxygen, sulfur, carbonyl, alkylene,. alkylcarbonyl, alkylamino, -C(=N-Oalkyl)-, NR 4 , -C(=O) NR 4 -, or -NR4C(=O)-; R 4 is hydrogen or alkyl; Cy 1 is aryl, cycloalkyl, cycloalkenyl, heteroaryl, or heterocycle; Z is a substituent R 6 or a group represented by -L 3 -Cy 3 ; R 6 is hydrogen, acyl, acyloxy, alkenyl, alkoxy, alkoxyalkoxy, alkoxyalkyl, alkoxycarbonyl, alkoxyimino, alkoxysulfonyl, alkyl, alkylcarbonyl, alkylsulfonyl, alkynyl, amido, carboxy, cyano, cycloalkyl, fiuoroalkoxy, haloalkoxy, haloalkyl, halogen, hydroxy, hydroxyalkyl, mercapto, nitro, alkylthio, amino, NHR 7 , NR 7 R 8 , -N(R 7 )C(=O)R 9 , -C(=O)NR 7 R 8 , or N(R 7 )SO 2 (R 10 ); L 3 is a bond, oxygen, sulfur, carbonyl, alkylene, alkylcarbonyl, alkylamino, -C(=N-Oalkyl)-, NR 11 , -C(=O) NR 11 -, or -NR 11 C(=O)-;Cy 3 is aryl, cycloalkyl, cycloalkenyl, heteroaryl, or heterocycle; R 7 , R 8 , R 9 , R 10 , and R 11 at each occurrence are independently hydrogen,C 1-4 alkyl, C 3 -C 4 cycloalkyl, or a (C 3 -C 4 cycloalkyl)amine; are useful in treating conditions or disorders prevented by or ameliorated by histamine-3 receptor ligands. Octahydro-pyrrolo[3,4-b]pyrrole compounds, methods for using such compounds, compositions for making them, and processes for preparing such compounds are disclosed herein.

公开(公告)号：WO2007100990A2

公开(公告)日：2007-09-07

申请号：PCT/US2007062329

申请日：2007-02-16

Applicant: ABBOTT LAB ,  COWART MARLON D ,  ZHAO CHEN ,  SUN MINGHUA ,  BLACK LAWRENCE A ,  ZHENG GUO ZHU ,  GREGG ROBERT J ,  ZHANG GEOFF G Z ,  SHEIKH AHMAD Y ,  LOU XIAOCHUN ,  HENRY RODGER F ,  BARNES DAVID M ,  KOLACZKOWSKI LAWRENCE ,  HAIGHT ANTHONY R ,  CHANG SOU-JEN ,  WITTENBERGER STEVEN J ,  FICKES MICHAEL G

Inventor： COWART MARLON D ,  ZHAO CHEN ,  SUN MINGHUA ,  BLACK LAWRENCE A ,  ZHENG GUO ZHU ,  GREGG ROBERT J ,  ZHANG GEOFF G Z ,  SHEIKH AHMAD Y ,  LOU XIAOCHUN ,  HENRY RODGER F ,  BARNES DAVID M ,  KOLACZKOWSKI LAWRENCE ,  HAIGHT ANTHONY R ,  CHANG SOU-JEN ,  WITTENBERGER STEVEN J ,  FICKES MICHAEL G

IPC: C07D487/04 ,  A61K31/407

CPC classification number: C07D487/04

Abstract: Octahydro-pyrrolo[3,4-b]pyrrole derivatives are useful in treating conditions or disorders prevented by or ameliorated by histamine-3 receptor ligands. Octahydro-pyrrolo[3,4-b]pyrrole compounds, methods for using such compounds, compositions for making them, and processes for preparing such compounds are disclosed herein.

Abstract translation: 八氢吡咯并[3,4-b]吡咯衍生物可用于治疗组胺-3受体配体预防或改善的病症或病症。 八氢吡咯并[3,4-b]吡咯化合物，使用这些化合物的方法，制备它们的组合物和制备这些化合物的方法在本文中公开。

公开(公告)号：WO2010051030A1

公开(公告)日：2010-05-06

申请号：PCT/US2009/005897

申请日：2009-10-30

Applicant: BIOGEN IDEC MA INC. ,  GUCKIAN, Kevin, M. ,  CALDWELL, Richard, D. ,  KUMARAVEL, Gnanasambandam ,  LEE, Wen-cherng ,  LIN, Edward, Yin-shiang ,  LIU, Xiaogao ,  MA, Bin ,  SCOTT, Daniel, M. ,  SHI, Zhan ,  ZHENG, Guo, Zhu ,  TAVERAS, Arthur, G. ,  THOMAS, Jermaine

Inventor： GUCKIAN, Kevin, M. ,  CALDWELL, Richard, D. ,  KUMARAVEL, Gnanasambandam ,  LEE, Wen-cherng ,  LIN, Edward, Yin-shiang ,  LIU, Xiaogao ,  MA, Bin ,  SCOTT, Daniel, M. ,  SHI, Zhan ,  ZHENG, Guo, Zhu ,  TAVERAS, Arthur, G. ,  THOMAS, Jermaine

IPC: A01N47/10 ,  A61K31/27 ,  A61K31/135

CPC classification number: A61K31/135 ,  A61K31/27 ,  C07C205/26 ,  C07C205/50 ,  C07C217/52 ,  C07C217/60 ,  C07C229/32 ,  C07C271/16 ,  C07D263/38 ,  C07F9/091 ,  C07F9/093 ,  C07F9/653 ,  C07F9/65744

Abstract: Compounds that have agonist activity at one or more of the SlP receptors are provided. The compounds are sphingosine analogs that, after phosphorylation, can behave as agonists at S lP receptors.

Abstract translation: 提供了在一种或多种S1P受体上具有激动剂活性的化合物。 这些化合物是鞘氨醇类似物，其在磷酸化之后可以作为S1P受体的激动剂。

公开(公告)号：WO2005007642A2

公开(公告)日：2005-01-27

申请号：PCT/US2004/021836

申请日：2004-07-09

Applicant: ABBOTT LABORATORIES ,  ZHENG, Guo Zhu ,  BROWN, Brian, S. ,  TURNER, Sean, C. ,  WHITE, Tammie, K. ,  SCHMIDT, Robert, G. ,  KOENIG, John, R. ,  LEE, Chih-Hung

Inventor： ZHENG, Guo Zhu ,  BROWN, Brian, S. ,  TURNER, Sean, C. ,  WHITE, Tammie, K. ,  SCHMIDT, Robert, G. ,  KOENIG, John, R. ,  LEE, Chih-Hung

IPC: C07D401/04

CPC classification number: C07D401/04 ,  C07D487/08

Abstract: The present invention relates to compounds of formula (I-VII) (I), or a pharmaceutically acceptable salt or prodrug thereof, in which A, L, R 6 , R 7 and R 8 are defined herein. The present invention also relates to methods of trating pain using these compounds and pharmaceutical compositions including these compounds.

Abstract translation: 本发明涉及式（I-VII）（I）化合物或其药学上可接受的盐或前药，其中A，L，R 6，R 7和R 8如本文所定义。 本发明还涉及使用这些化合物和包括这些化合物的药物组合物来治疗疼痛的方法。

公开(公告)号：WO2019199667A3

公开(公告)日：2019-10-17

申请号：PCT/US2019/026313

申请日：2019-04-08

Applicant: KEANEY, Gregg F. ,  WANG, John ,  GERARD, Baudouin ,  ARAI, Kenzo ,  LIU, Xiang ,  ZHENG, Guo Zhu ,  KIRA, Kazunobu ,  MARCAURELLE, Lisa A. ,  NEVALAINEN, Marta ,  HAO, Ming-Hong ,  O'SHEA, Morgan Welzel ,  TIVITMAHAISOON, Parcharee ,  PRAJAPATI, Sudeep ,  LUO, Touping ,  GEARHART, Nicholas C. ,  LOWE, Jason T. ,  KOTAKE, Yoshihiko ,  NAGAO, Satoshi ,  KANADA SONOBE, Regina Mikie ,  MIYANO, Masayuki ,  MURAI, Norio ,  COOK, Andrew ,  ELLERY, Shelby ,  ENDO, Atsushi ,  PALACINO, James ,  REYNOLDS, Dominic

Inventor： KEANEY, Gregg F. ,  WANG, John ,  GERARD, Baudouin ,  ARAI, Kenzo ,  LIU, Xiang ,  ZHENG, Guo Zhu ,  KIRA, Kazunobu ,  MARCAURELLE, Lisa A. ,  NEVALAINEN, Marta ,  HAO, Ming-Hong ,  O'SHEA, Morgan Welzel ,  TIVITMAHAISOON, Parcharee ,  PRAJAPATI, Sudeep ,  LUO, Touping ,  GEARHART, Nicholas C. ,  LOWE, Jason T. ,  KOTAKE, Yoshihiko ,  NAGAO, Satoshi ,  KANADA SONOBE, Regina Mikie ,  MIYANO, Masayuki ,  MURAI, Norio ,  COOK, Andrew ,  ELLERY, Shelby ,  ENDO, Atsushi ,  PALACINO, James ,  REYNOLDS, Dominic

IPC: C07D313/00 ,  C07D407/12 ,  C07D407/14 ,  A61K31/497 ,  A61K31/4427 ,  A61K31/365 ,  A61P35/00

Abstract: The present disclosure provides novel pladienolide compounds, pharmaceutical compositions containing such compounds, and methods for using the compounds as therapeutic agents. These compounds may be useful in the treatment of cancers, particularly cancers in which agents that target the spliceosome and mutations therein are known to be useful. Also provided herein are methods of treating cancers by administering at least one compound disclosed herein and at least one additional therapy.