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公开(公告)号：US20230293519A1
公开(公告)日：2023-09-21
申请号：US17966717
申请日：2022-10-14
发明人： Eric LEFEBVRE , Gregory P. COSGROVE
IPC分类号： A61K31/506 , A61K31/517 , A61K31/519 , A61K31/501 , A61K31/502 , A61K31/4375 , A61P11/00
CPC分类号： A61K31/506 , A61K31/4375 , A61K31/501 , A61K31/502 , A61K31/517 , A61K31/519 , A61P11/00
摘要： The invention relates to methods of treating a subject for a disease comprising administration of compounds of Formula (A), Formula (I), or Formula (II):
or a salt thereof, wherein R1, R2, R10, R11, R12, R13, R14, R15, R16, q and p are as described herein; and administering to the subject at least a second drug selected from pirfenidone and nintedanib, or a salt thereof. Compounds of Formula (A), Formula (I), Formula (II), and pharmaceutical compositions thereof are αvβ6 integrin inhibitors that are useful for treating fibrosis such as idiopathic pulmonary fibrosis (IPF) and nonspecific interstitial pneumonia (NSIP).-
公开(公告)号：US20230117605A1
公开(公告)日：2023-04-20
申请号：US17869758
申请日：2022-07-20
发明人： Martin DECARIS , Scott TURNER , Eric LEFEBVRE
IPC分类号： A61K31/5025 , A61K31/502 , A61P11/00 , A61K9/00 , A61K31/4375
摘要： The invention relates to dosage forms for daily administration of compounds of formula (A) and formula (I): or a salt thereof, wherein R1, R2, R10, R11, R12, R13, R14, R15, R16, q and p are as described herein. Compounds of formula (A), formula (I), and pharmaceutical compositions thereof are αvβ6 integrin inhibitors that are useful for treating fibrosis such as idiopathic pulmonary fibrosis (IPF) and nonspecific interstitial pneumonia (NSIP).
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公开(公告)号：US20220289743A1
公开(公告)日：2022-09-15
申请号：US17679002
申请日：2022-02-23
发明人： Katerina LEFTHERIS , Maureen REILLY , Darren FINKELSTEIN , Nicole COOPER , Christopher BAILEY , Jacob CHA
IPC分类号： C07D471/04 , C07D519/00
摘要： The invention relates to compounds of formula (A): or a salt thereof, wherein R1, R2, R5a, R5b, R6a, R6b, R7a, R7b, R8a, R8b, R9a, R9b, R10a, R10b, R11a, R11b, R21, n, and G are as described herein. Compounds of formula (I) and pharmaceutical compositions thereof are αvβ6 integrin inhibitors that are useful for treating fibrosis such as idiopathic pulmonary fibrosis (IPF) and nonspecific interstitial pneumonia (NSIP).
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公开(公告)号：US11180494B2
公开(公告)日：2021-11-23
申请号：US16596649
申请日：2019-10-08
发明人： Jacob Cha , Manuel Munoz , Maureen Reilly , Nicole Cooper , Katerina Leftheris , David J. Morgans, Jr. , Timothy Hom , Yajun Zheng
IPC分类号： A61K31/4375 , C07D471/04 , C07D519/00
摘要： The invention relates to compounds of formula (I): or a salt thereof, wherein R1, G, L1, L2, L3, and Y are as described herein. Compounds of formula (I) and pharmaceutical compositions thereof are inhibitors of one, or both of, αvβ1 integrin and αvβ6 integrin that are useful for treating fibrosis such as in nonalcoholic steatohepatitis (NASH), idiopathic pulmonary fibrosis (IPF) and nonspecific interstitial pneumonia (NSIP).
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公开(公告)号：US20210122747A1
公开(公告)日：2021-04-29
申请号：US16894712
申请日：2020-06-05
发明人： David John MORGANS, Jr. , Randall L. HALCOMB , Gustave BERGNES , Hui LI , Lan JIANG , Jacob CHA , Timothy HOM
IPC分类号： C07D471/04
摘要： The invention relates to compounds of formula (I): or a salt thereof, wherein R1, R5, R7, R8. X, m, n, p and q are as described herein. Compounds of formula (I) and pharmaceutical compositions thereof are αvβ6 integrin inhibitors that are useful for treating tissue specific fibrosis such as idiopathic pulmonary fibrosis (IPF) and nonspecific interstitial pneumonia (NSIP).
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公开(公告)号：US20240350494A1
公开(公告)日：2024-10-24
申请号：US18688267
申请日：2022-09-01
IPC分类号： A61K31/517 , A61K49/00 , A61P11/00
CPC分类号： A61K31/517 , A61K49/0004 , A61P11/00
摘要： The invention relates methods of determining therapeutic doses for conditions mediated by integrin and methods of therapy for conditions mediated by integrin comprising administering an integrin modulating compound in an amount that achieves receptor occupancy of the integrin. The invention further relates to dosage forms for daily administration of integrin modulating compounds that are useful for treating conditions mediated by at least one integrin including, e.g., fibrosis such as idiopathic pulmonary fibrosis (IFF) and nonspecific interstitial pneumonia (NSIP).
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公开(公告)号：US20240270742A1
公开(公告)日：2024-08-15
申请号：US18545952
申请日：2023-12-19
发明人： Jacob CHA , Manuel MUÑOZ , Maureen REILLY , Nicole COOPER , Katerina LEFTHERIS , David J. MORGANS, JR. , Timothy HOM , Yajun ZHENG , Christopher BAILEY , Darren FINKELSTEIN
IPC分类号： C07D471/04 , C07D519/00
CPC分类号： C07D471/04 , C07D519/00
摘要： The invention relates to compounds of formula (I):
or a salt thereof, wherein R1, G, L1, L2, L3, and Y are as described herein. Compounds of formula (I) and pharmaceutical compositions thereof are inhibitors of one, or both of, αvβ1 integrin and αvβ6 integrin that are useful for treating fibrosis such as in nonalcoholic steatohepatitis (NASH), idiopathic pulmonary fibrosis (IPF) and nonspecific interstitial pneumonia (NSIP).-
公开(公告)号：US11673887B2
公开(公告)日：2023-06-13
申请号：US16809244
申请日：2020-03-04
发明人： Lan Jiang , David John Morgans, Jr. , Gustave Bergnes , Chun Chen , Hui Li , Patrick Andre , Randall Halcomb , Jacob Cha , Timothy Hom
IPC分类号： C07D471/04 , C07D213/74 , C07D233/70 , C07D233/88 , C07D241/06 , C07D241/08 , C07D263/28 , C07D265/08 , C07D277/18 , C07D279/06 , C07D498/04 , A61P1/00 , A61P1/16 , A61P9/00 , A61P11/00 , A61P13/12 , A61P17/00
CPC分类号： C07D471/04 , A61P1/00 , A61P1/16 , A61P9/00 , A61P11/00 , A61P13/12 , A61P17/00 , C07D213/74 , C07D233/70 , C07D233/88 , C07D241/06 , C07D241/08 , C07D263/28 , C07D265/08 , C07D277/18 , C07D279/06
摘要： The invention relates to compounds of formula (I):
or a salt thereof, wherein R1, A, L, and R2 and n are as described herein. Compounds of formula (I) and pharmaceutical compositions thereof are αvβ1 integrin inhibitors that are useful for treating tissue specific fibrosis.-
公开(公告)号：US20230060422A1
公开(公告)日：2023-03-02
申请号：US17786491
申请日：2020-12-18
发明人： Kraig ANDERSON , Christopher BAILEY , Avirup BOSE , Jacob CHA , Nicole COOPER , Darren FINKELSTEIN , Linda GREENBAUM , Johannes HULL , Susan Caroline KIRKLAND , Katerina LEFTHERIS , Maureen REILLY , Peter TARSA , Chinweike UKOMADU
IPC分类号： A61K31/4162 , A61K31/4375 , A61K31/7048 , A61K45/06 , A61P1/16
摘要： The invention provides a pharmaceutical combination including an αvβ1 integrin inhibitor and at least one additional therapeutic agent for preventing, delaying or treating liver diseases or disorders. The additional therapeutic agent may be an SGLT1/2 inhibitor, among a diverse selection of agents. For example, the pharmaceutical combination includes (S)-2-(4-methyltetrahydro-2H-pyran-4-carboxamido)-9-(5,6,7,8-tetrahydro-1,8-naphthyridin-2-yl) nonanoic acid (Compound 1) and at least one additional therapeutic agent.
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公开(公告)号：US20210017171A1
公开(公告)日：2021-01-21
申请号：US16914209
申请日：2020-06-26
发明人： Jacob CHA , Chengguo DONG , Timothy HOM , Lan JIANG , Katerina LEFTHERIS , Hui LI , David John MORGANS, JR. , Manuel MUNOZ , Maureen REILLY , Yajun ZHENG
IPC分类号： C07D471/04 , C07D519/00
摘要： The invention relates to compounds of formula (A) and formula (I): or a salt thereof, wherein R1, R2, R10, R11, R12, R13, R14, R15, R16, q and p are as described herein. Compounds of formula (A), formula (I), and pharmaceutical compositions thereof are αvβ6 integrin inhibitors that are useful for treating fibrosis such as idiopathic pulmonary fibrosis (IPF) and nonspecific interstitial pneumonia (NSIP).
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