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公开(公告)号：US20220213026A1
公开(公告)日：2022-07-07
申请号：US17431091
申请日：2020-02-14
发明人： Dean A. Wacker , Susheel Jethanand Nara , Srinivas Cheruku , Kandhasamy Sarkunam , Firoz Ali Jaipuri , Soodamani Thangavel , Rishikesh Narayan , Subba Reddy Bandreddy , Srinivas Jogi , Pavan Kalyan Kathi
IPC分类号： C07C233/61 , C07D295/04 , C07D207/06 , C07D205/04 , C07D309/04 , C07D405/14 , C07D271/06 , C07D277/64 , C07D413/04 , C07D405/04
摘要： Disclosed are compounds of Formula (I) or a stereoisomer, a tautomer, or a pharmaceutically acceptable salt or solvate thereof, wherein Q is a 5-membered heterocyclyl or 5-membered heteroaryl having 1 to 4 heteroatoms independently selected from N, O, and S, substituted with zero to 4 R1; and A, X1, X2, X3, X4, Z1, Z2, R1, R2, R3a, R3b, a, b, and d are defined herein. Also disclosed are methods of using these compounds to modulate the activity of farnesoid X receptor (FXR); pharmaceutical compositions comprising these compounds; and methods of treating a disease, disorder, or condition associated with FXR dysregulation, such as pathological fibrosis, transplant rejection, cancer, osteoporosis, and inflammatory disorders, by using the compounds and pharmaceutical compositions.
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公开(公告)号：US11713312B2
公开(公告)日：2023-08-01
申请号：US17544490
申请日：2021-12-07
发明人： Dean A. Wacker , Susheel Jethanand Nara , Srinivas Cheruku , Kandhasamy Sarkunam , Firoz Ali Jaipuri , Soodamani Thangavel , Srinivas Jogi , Pavan Kalyan Kathi
IPC分类号： C07D413/12 , C07D271/06 , A61P11/00
CPC分类号： C07D413/12 , A61P11/00 , C07D271/06
摘要： Disclosed are compounds of Formula (I):
or a stereoisomer, a tautomer, or a salt or solvate thereof, wherein all the variables are as defined herein. These compounds modulate the activity of farnesoid X receptor (FXR), for example, as agonists. Also disclosed are pharmaceutical compositions comprising these compounds and methods of treating a disease, disorder, or condition associated with FXR dysregulation, such as pathological fibrosis, transplant rejection, cancer, osteoporosis, and inflammatory disorders, by using the compounds and pharmaceutical compositions.-
公开(公告)号：US12030835B2
公开(公告)日：2024-07-09
申请号：US17431091
申请日：2020-02-14
发明人： Dean A. Wacker , Susheel Jethanand Nara , Srinivas Cheruku , Kandhasamy Sarkunam , Firoz Ali Jaipuri , Soodamani Thangavel , Rishikesh Narayan , Subba Reddy Bandreddy , Srinivas Jogi , Pavan Kalyan Kathi
IPC分类号： C07C233/61 , C07D205/04 , C07D207/06 , C07D271/06 , C07D277/64 , C07D295/04 , C07D309/04 , C07D405/04 , C07D405/14 , C07D413/04
CPC分类号： C07C233/61 , C07D205/04 , C07D207/06 , C07D271/06 , C07D277/64 , C07D295/04 , C07D309/04 , C07D405/04 , C07D405/14 , C07D413/04
摘要： Disclosed are compounds of Formula (I) or a stereoisomer, a tautomer, or a pharmaceutically acceptable salt or solvate thereof, wherein Q is a 5-membered heterocyclyl or 5-membered heteroaryl having 1 to 4 heteroatoms independently selected from N, O, and S, substituted with zero to 4 R1; and A, X1, X2, X3, X4, Z1, Z2, R1, R2, R3a, R3b, a, b, and d are defined herein. Also disclosed are methods of using these compounds to modulate the activity of farnesoid X receptor (FXR); pharmaceutical compositions comprising these compounds; and methods of treating a disease, disorder, or condition associated with FXR dysregulation, such as pathological fibrosis, transplant rejection, cancer, osteoporosis, and inflammatory disorders, by using the compounds and pharmaceutical compositions.
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公开(公告)号：US20220162201A1
公开(公告)日：2022-05-26
申请号：US17431006
申请日：2020-02-14
发明人： Dean A. Wacker , Susheel Jethanand Nara , Srinivas Cheruku , Kandhasamy Sarkunam , Firoz Ali Jaipuri , Rishikesh Narayan , Subba Reddy Bandreddy , Srinivas Jogi
IPC分类号： C07D413/12 , C07D413/14 , C07D417/12 , C07D403/12 , C07D217/06 , C07D271/06 , C07D417/14
摘要： Disclosed are compounds of Formula (I): or a stereoisomer, a tautomer, or a salt or solvate thereof, wherein Q is C2-6 alkenyl or C2-6 alkynyl, each substituted with zero to 2 R1; and the other variables are as defined herein. These compounds modulate the activity of farnesoid X receptor (FXR), for example, as agonists. Also disclosed are pharmaceutical compositions comprising these compounds and methods of treating a disease, disorder, or condition associated with FXR dysregulation, such as pathological fibrosis, transplant rejection, cancer, osteoporosis, and inflammatory disorders, by using the compounds and pharmaceutical compositions.
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公开(公告)号：US20220081430A1
公开(公告)日：2022-03-17
申请号：US17430903
申请日：2020-02-14
发明人： Dean A. Wacker , Susheel Jethanand Nara , Srinivas Cheruku , Kandhasamy Sarkunam , Firoz Ali Jaipuri , Soodamani Thangavel , Rishikesh Narayan , Srinivas Jogi , Pavan Kalyan Kathi
IPC分类号： C07D413/12 , C07D401/12 , C07D271/06 , C07D213/26 , C07D417/12
摘要： Disclosed are compounds of Formula (I): or a stereoisomer, a tautomer, or a pharmaceutically acceptable salt or solvate thereof, when Q is: (i) halo, cyano, hydroxyl, NRxRx, C(O)OH, C(O)NH2, C1-6 alkyl substiuted with zero to 6 R1a, or P(O)R1cR1c, or (ii) L R1; and A, X1, X2, X3, X4, Z1, Z2, R1, R1a, R1c, R2, R3a, R3b, Rx, L, a, b, and d are defined herein. Also disclosed are methods of using these compounds to modulate the activity of farnesoid X receptor (FXR); pharmaceutical compositions comprising these compounds; and methods of treating a disease, disorder, or condition associated with FXR dysregulation, such as pathological fibrosis, transplant rejection, cancer, osteoporosis, and inflammatory disorders, by using the compounds and pharmaceutical compositions.
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公开(公告)号：US11254663B2
公开(公告)日：2022-02-22
申请号：US16789551
申请日：2020-02-13
发明人： Dean A. Wacker , Susheel Jethanand Nara , Srinivas Cheruku , Kandhasamy Sarkunam , Firoz Ali Jaipuri , Soodamani Thangavel , Srinivas Jogi , Pavan Kalyan Kathi
IPC分类号： C07D413/12 , C07D271/06 , A61P11/00
摘要： Disclosed are compounds of Formula (I): or a stereoisomer, a tautomer, or a salt or solvate thereof, wherein all the variables are as defined herein. These compounds modulate the activity of farnesoid X receptor (FXR), for example, as agonists. Also disclosed are pharmaceutical compositions comprising these compounds and methods of treating a disease, disorder, or condition associated with FXR dysregulation, such as pathological fibrosis, transplant rejection, cancer, osteoporosis, and inflammatory disorders, by using the compounds and pharmaceutical compositions.
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公开(公告)号：US20210261535A1
公开(公告)日：2021-08-26
申请号：US16789551
申请日：2020-02-13
发明人： Dean A. Wacker , Susheel Jethanand Nara , Srinivas Cheruku , Kandhasamy Sarkunam , Firoz Ali Jaipuri , Soodamani Thangavel , Rishikesh Narayan , Subba Reddy Bandreddy , Srinivas Jogi , Pavan Kalyan Kathi
IPC分类号： C07D413/12 , C07D271/06 , A61P11/00
摘要： Disclosed are compounds of Formula (I): or a stereoisomer, a tautomer, or a salt or solvate thereof, wherein all the variables are as defined herein. These compounds modulate the activity of farnesoid X receptor (FXR), for example, as agonists. Also disclosed are pharmaceutical compositions comprising these compounds and methods of treating a disease, disorder, or condition associated with FXR dysregulation, such as pathological fibrosis, transplant rejection, cancer, osteoporosis, and inflammatory disorders, by using the compounds and pharmaceutical compositions.
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