公开(公告)号：WO2020249957A1

公开(公告)日：2020-12-17

申请号：PCT/GB2020/051415

申请日：2020-06-12

Applicant: ENTERPRISE THERAPEUTICS LIMITED

Inventor： COLLINGWOOD, Stephen ,  MCCARTHY, Clive ,  HAY, Duncan, Alexander ,  HARGRAVE, Jonathan, David ,  MA, Albert ,  SCHOFIELD, Thomas, Beauregard ,  SMITH, Matthew ,  WALKER, Edward ,  WENT, Naomi ,  INGRAM, Peter ,  STIMSON, Christopher ,  KHOR, Someina

IPC: C07D231/56 ,  C07D235/08 ,  C07D235/12 ,  C07D235/14 ,  C07D263/56 ,  C07D405/06 ,  C07D413/10 ,  C07D471/04 ,  A61P11/12 ,  A61K31/437 ,  A61K31/416 ,  A61K31/4184 ,  A61K31/423

Abstract: Compounds of general formula (I) and their tautomeric forms all enantiomers and isotopic variants and salts and solvates thereof: Formula (I), wherein (AA) represents a single or a double bond and R 1 , R 2 , X 1 , X 2 , X 3 , X 4 , X 5 , Y and Z are as defined herein; are useful for treating respiratory disease and other diseases and conditions modulated by TMEM16A.

公开(公告)号：WO2019145726A9

公开(公告)日：2019-08-01

申请号：PCT/GB2019/050209

申请日：2019-01-25

Applicant: ENTERPRISE THERAPEUTICS LIMITED

Inventor： COLLINGWOOD, Stephen ,  MCCARTHY, Clive ,  HARGRAVE, Jonathan, David ,  HAY, Duncan, Alexander ,  SCHOFIELD, Thomas, Beauregard ,  ELLAM, Sarah ,  BUXTON, Craig ,  HABGOOD, Matthew ,  INGRAM, Peter ,  MA, Chun Yan ,  NAPIER, Spencer ,  SHAIKH, Abdul ,  SMITH, Matthew ,  STIMSON, Christopher ,  WALKER, Edward

IPC: C07D213/72 ,  C07D309/10 ,  C07C1/00 ,  C07D401/12 ,  C07D405/12 ,  C07D413/12 ,  C07D417/12 ,  A61P11/00

Abstract: Compounds of general formula (I): wherein R 1 , R 2 , R 3 , R 4 , R 5a , R 5b X 1 , X 2 , Z and Y are as defined herein are positive modulators of the calcium-activated chloride channel (CaCC), TMEM16A. The compounds are useful for treating diseases and conditions affected by modulation of TMEM16A, particularly respiratory diseases and conditions.

公开(公告)号：WO2018096325A1

公开(公告)日：2018-05-31

申请号：PCT/GB2017/053499

申请日：2017-11-22

Applicant: ENTERPRISE THERAPEUTICS LIMITED

Inventor： MCCARTHY, Clive ,  HARGRAVE, Jonathan, David ,  HAY, Duncan, Alexander ,  SCHOFIELD, Thomas, Beauregard ,  WENT, Naomi

IPC: C07D487/04 ,  A61P11/12 ,  A61K31/4985

Abstract: Compounds of general formula (I) wherein R 1 , R 2 , R 3 , R 4 , R 5 and X are as defined herein are inhibitors of the epithelial sodium channel (ENaC) and are useful for the treatment or prevention respiratory diseases and conditions, skin conditions and ocular conditions.

公开(公告)号：WO2021014172A1

公开(公告)日：2021-01-28

申请号：PCT/GB2020/051785

申请日：2020-07-24

Applicant: ENTERPRISE THERAPEUTICS LIMITED

Inventor： COLLINGWOOD, Stephen, Paul ,  BUXTON, Craig ,  HABGOOD, Matthew ,  HARGRAVE, Jonathan, David ,  SCHOFIELD, Thomas, Beauregard ,  SMITH, Matthew ,  STIMSON, Christopher

IPC: C07D401/12 ,  C07D401/14 ,  A61P11/00 ,  A61K31/44

Abstract: Compounds of general formula (I), wherein R 1 , R 2 , R 3 , R 4 , R 5 , X 1 , X 2 and X 3 are as defined herein are useful for treating respiratory disease and other diseases and conditions modulated by TMEM16A.

公开(公告)号：WO2021014166A1

公开(公告)日：2021-01-28

申请号：PCT/GB2020/051778

申请日：2020-07-24

Applicant: ENTERPRISE THERAPEUTICS LIMITED

Inventor： COLLINGWOOD, Stephen, Paul ,  BUXTON, Craig ,  HARGRAVE, Jonathan, David ,  INGRAM, Peter ,  SCHOFIELD, Thomas, Beauregard ,  SHAIKH, Abdul ,  STIMSON, Christopher

IPC: A61P11/00 ,  A61K31/44 ,  C07D213/81 ,  C07D405/12

Abstract: Compounds of general formula (I), wherein R 1 , R 2 , R 3 , R 4 , R 5 , R 6 , R 7 , R 8 , R 9 and R 10 are as defined herein are useful for treating respiratory disease and other diseases and conditions modulated by TMEM16A.

公开(公告)号：WO2020249956A1

公开(公告)日：2020-12-17

申请号：PCT/GB2020/051414

申请日：2020-06-12

Applicant: ENTERPRISE THERAPEUTICS LIMITED

Inventor： COLLINGWOOD, Stephen ,  HARGRAVE, Jonathan, David ,  HAY, Duncan, Alexander ,  WALKER, Edward

IPC: A61P11/00 ,  C07C237/42 ,  C07D213/81 ,  C07D213/82 ,  C07D333/38 ,  A61K31/44 ,  A61K31/381 ,  A61K31/167 ,  A61K31/166 ,  C07C233/43 ,  C07C233/54 ,  C07D333/40 ,  C07D333/54 ,  C07C233/73 ,  C07C235/38

Abstract: Compounds of general formula (I), which are useful for treating respiratory disease and other diseases and conditions modulated by TMEM16A. wherein A is defined as Formula.

公开(公告)号：WO2019145726A1

公开(公告)日：2019-08-01

申请号：PCT/GB2019/050209

申请日：2019-01-25

Applicant: ENTERPRISE THERAPEUTICS LIMITED

Inventor： COLLINGWOOD, Stephen ,  MCCARTHY, Clive ,  HARGRAVE, Jonathan, David ,  HAY, Duncan, Alexander ,  SCHOFIELD, Thomas, Beauregard ,  ELLAM, Sarah ,  BUXTON, Craig ,  HABGOOD, Matthew ,  INGRAM, Peter ,  MA, Chun Yan ,  NAPIER, Spencer ,  SHAIKH, Abdul ,  SMITH, Matthew ,  STIMSON, Christopher ,  WALKER, Edward

IPC: C07D213/72 ,  C07D309/10 ,  C07C1/00 ,  C07D401/12 ,  C07D405/12 ,  C07D413/12 ,  C07D417/12 ,  A61P11/00

Abstract: Compounds of general formula (I): wherein R 1 , R 2 , R 3 , R 4 , R 5a , R 5b X 1 , X 2 , Z and Y are as defined herein are positive modulators of the calcium-activated chloride channel (CaCC), TMEM16A. The compounds are useful for treating diseases and conditions affected by modulation of TMEM16A, particularly respiratory diseases and conditions.