公开(公告)号：WO2021127586A1

公开(公告)日：2021-06-24

申请号：PCT/US2020/066243

申请日：2020-12-18

Applicant: CALICO LIFE SCIENCES LLC ,  ABBVIE INC. ,  VEITS, Gesine Kerstin ,  FITZGERALD, Mark E. ,  HIRD, Alexander W. ,  HENDERSON, James A. ,  VORA, Harit U. ,  SWEIS, Ramzi F. ,  KORT, Michael E. ,  NASVESCHUK, Christopher G. ,  DUPLESSIS, Martin

Inventor： VEITS, Gesine Kerstin ,  FITZGERALD, Mark E. ,  HIRD, Alexander W. ,  HENDERSON, James A. ,  VORA, Harit U. ,  SWEIS, Ramzi F. ,  NASVESCHUK, Christopher G. ,  DUPLESSIS, Martin

IPC: C07D417/12 ,  C07D417/14 ,  C07D471/10 ,  A61P3/00 ,  A61P35/00 ,  A61K47/00 ,  A61K31/4523 ,  A61K31/4525 ,  A61K31/454 ,  A61K31/4545 ,  A61K9/0019

Abstract: Provided herein are compounds, compositions, and methods useful for degrading protein tyrosine phosphatase, e.g., protein tyrosine phosphatase non-receptor type 2 (PTPN2) and/or protein tyrosine phosphatase non-receptor type 1 (PTPN1), and for treating related diseases favorably responsive to PTPN1 or PTPN2 inhibitor treatment, e.g., a cancer 5 or a metabolic disease.

公开(公告)号：WO2012142457A2

公开(公告)日：2012-10-18

申请号：PCT/US2012033586

申请日：2012-04-13

Applicant: BROAD INST INC ,  MUNOZ BENITO ,  BEAUDOIN JENNIFER ,  COMER EAMON ,  LEE MAURICE DUPONT ,  DUVALL JEREMY ,  FITZGERALD MARK E ,  FOLEY MICHAEL ,  HEIDEBRECHT RICHARD W ,  MARCAURELLE LISA ,  MASI DANIELA ,  MERCIER MARION ,  MULROONEY CAROL ,  MUNCIPINTO GIOVANNI ,  ROWLEY ANN

Inventor： MUNOZ BENITO ,  BEAUDOIN JENNIFER ,  COMER EAMON ,  LEE MAURICE DUPONT ,  DUVALL JEREMY ,  FITZGERALD MARK E ,  FOLEY MICHAEL ,  HEIDEBRECHT RICHARD W ,  MARCAURELLE LISA ,  MASI DANIELA ,  MERCIER MARION ,  MULROONEY CAROL ,  MUNCIPINTO GIOVANNI ,  ROWLEY ANN

IPC: C07D273/01 ,  A61K31/553 ,  A61P33/00

CPC classification number: A61K31/553 ,  C07D273/01 ,  C07D409/12 ,  C07D413/06 ,  C07D413/12 ,  C07D498/04

Abstract: The present invention relates to a macrolactam compound, and methods for treating a subject with malaria using the macrolactam compound, represented by the following structural formula (l), wherein the values and preferred values of the variables are defined herein.

Abstract translation: 本发明涉及一种大分子内酰胺化合物，以及使用由以下结构式（1）表示的大环内酰胺化合物用疟疾治疗受试者的方法，其中变量的值和优选值在本文中定义。

公开(公告)号：WO2013049585A1

公开(公告)日：2013-04-04

申请号：PCT/US2012/057942

申请日：2012-09-28

Applicant: HENGRUI (USA), LTD. ,  SMITH, Emilie, D. ,  FITZGERALD, Mark, E. ,  JIANG, Rong ,  ATKINSON, Robert, N. ,  VEAL, James, M. ,  HUANG, Kenneth, H.

Inventor： SMITH, Emilie, D. ,  FITZGERALD, Mark, E. ,  JIANG, Rong ,  ATKINSON, Robert, N. ,  VEAL, James, M. ,  HUANG, Kenneth, H.

IPC: C07D513/04 ,  A61K31/429 ,  A61P3/00

CPC classification number: C07D513/04

Abstract: This disclosure relates to compounds, compositions and methods for the treatment of various disorders. In particular, the disclosure relates to thiazolotriazole and thiazoloimidazole compounds which agonize the activity of the protein TGR5. Formula (I)

Abstract translation: 本公开涉及用于治疗各种疾病的化合物，组合物和方法。 特别地，本公开涉及激活蛋白TGR5的活性的噻唑并三唑和噻唑并咪唑化合物。 式（I）

公开(公告)号：WO2012142457A3

公开(公告)日：2013-02-07

申请号：PCT/US2012033586

申请日：2012-04-13

Applicant: BROAD INST INC ,  MUNOZ BENITO ,  BEAUDOIN JENNIFER ,  COMER EAMON ,  LEE IV MAURICE DUPONT ,  DUVALL JEREMY ,  FITZGERALD MARK E ,  FOLEY MICHAEL ,  HEIDEBRECHT RICHARD W ,  MARCAURELLE LISA ,  MASI DANIELA ,  MERCIER MARION ,  MULROONEY CAROL ,  MUNCIPINTO GIOVANNI ,  ROWLEY ANN

Inventor： MUNOZ BENITO ,  BEAUDOIN JENNIFER ,  COMER EAMON ,  LEE IV MAURICE DUPONT ,  DUVALL JEREMY ,  FITZGERALD MARK E ,  FOLEY MICHAEL ,  HEIDEBRECHT RICHARD W ,  MARCAURELLE LISA ,  MASI DANIELA ,  MERCIER MARION ,  MULROONEY CAROL ,  MUNCIPINTO GIOVANNI ,  ROWLEY ANN

IPC: C07D273/01 ,  A61K31/553 ,  A61P33/00

CPC classification number: A61K31/553 ,  C07D273/01 ,  C07D409/12 ,  C07D413/06 ,  C07D413/12 ,  C07D498/04

Abstract: The present invention relates to a macrolactam compound, and methods for treating a subject with malaria using the macrolactam compound, represented by structural formula (l), wherein the values and preferred values of the variables are defined herein.

Abstract translation: 本发明涉及一种大环内酰胺化合物，以及使用由结构式（1）表示的大分子内酰胺化合物用疟疾治疗受试者的方法，其中变量的值和优选值在本文中定义。

公开(公告)号：WO2012142457A8

公开(公告)日：2012-10-18

申请号：PCT/US2012/033586

申请日：2012-04-13

Applicant: THE BROAD INSTITUTE, INC. ,  MUNOZ, Benito ,  BEAUDOIN, Jennifer ,  COMER, Eamon ,  LEE, IV, Maurice, Dupont ,  DUVALL, Jeremy ,  FITZGERALD, Mark, E. ,  FOLEY, Michael ,  HEIDEBRECHT, Richard, W. ,  MARCAURELLE, Lisa ,  MASI, Daniela ,  MERCIER, Marion ,  MULROONEY, Carol ,  MUNCIPINTO, Giovanni ,  ROWLEY, Ann

Inventor： MUNOZ, Benito ,  BEAUDOIN, Jennifer ,  COMER, Eamon ,  LEE, IV, Maurice, Dupont ,  DUVALL, Jeremy ,  FITZGERALD, Mark, E. ,  FOLEY, Michael ,  HEIDEBRECHT, Richard, W. ,  MARCAURELLE, Lisa ,  MASI, Daniela ,  MERCIER, Marion ,  MULROONEY, Carol ,  MUNCIPINTO, Giovanni ,  ROWLEY, Ann

IPC: C07D273/01 ,  A61K31/553 ,  A61P33/00

Abstract: The present invention relates to a macrolactam compound, and methods for treating a subject with malaria using the macrolactam compound, represented by structural formula (l), wherein the values and preferred values of the variables are defined herein.