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公开(公告)号:US11524930B2
公开(公告)日:2022-12-13
申请号:US16780316
申请日:2020-02-03
发明人: Boulos Zacharie , Shaun Abbott , Lyne Gagnon , Pierre Laurin , Brigitte Grouix
IPC分类号: C07C53/134 , C07C57/30 , C07C57/58 , A61K31/192 , C07C59/52
摘要: The present invention relates to compounds of: or a pharmaceutically acceptable salt thereof, wherein A is C5 alkyl, C6 alkyl, C5 alkenyl, C6 alkenyl, C(O)—(CH2)n—CH3 or CH(OH)—(CH2)n—CH3 wherein n is 3 or 4;
R1 is H, F or OH;
R2 is C5 alkyl, C6 alkyl, C5 alkenyl, C6 alkenyl, C(O)—(CH2)n—CH3 or CH(OH)—(CH2)n—CH3 wherein n is 3 or 4;
R3 is H, F, OH or CH2Ph;
R4 is H, F or OH;
Q is 1) (CH2)mC(O)OH wherein m is 1 or 2, 2) CH(CH3)C(O)OH, 3) C(CH3)2C(O)OH, 4) CH(F)—C(O)OH, 5) CF2—C(O)OH, or 6) C(O)—C(O)OH; and compositions comprising the same and the method using the same for the prevention or treatment of various fibrotic diseases and conditions in subjects, including pulmonary fibrosis, liver fibrosis, skin fibrosis, renal fibrosis, pancreas fibrosis, systemic sclerosis, cardiac fibrosis or macular degeneration.-
公开(公告)号:US20220016060A1
公开(公告)日:2022-01-20
申请号:US17311616
申请日:2019-12-05
发明人: LYNE GAGNON , PIERRE LAURIN , FRANK CESARI
摘要: Methods, formulations/compositions and uses for improving at least one of liver histology, heart histology, kidney histology, adipose tissue histology and a metabolic parameter in a patient suffering from Alström syndrome are described, comprising administration of a pharmaceutical oral formulation comprising 2-(3-pentylphenyl)acetate or a pharmaceutically salt thereof and a pharmaceutically acceptable excipient at a daily dose of about 500 mg to about 1500 mg. The treatment is preferably for a period of more than 48 weeks and is not interrupted for 15 days or more.
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公开(公告)号:US20230113202A1
公开(公告)日:2023-04-13
申请号:US17649752
申请日:2022-02-02
发明人: Shaun ABBOTT , Mylène DeLESELEUC , Julien MARTEL , Elyse BOURQUE , Jeremy GREEN , Alexandre LARIVÉE , Jean-Benoìt GIGUÈRE , Elodie LANDAGARAY , Claudio STURINO , Nadia Michel NASSER
IPC分类号: C07D405/06 , C07D405/14 , C07D413/06 , C07D409/14 , C07D405/12 , C07D249/06 , C07D487/10 , C07D471/10 , C07D471/08 , C07D401/14 , C07D491/056 , C07D409/06
摘要: The present invention provides compounds, compositions thereof, and methods of using the same for the inhibition of GPR84, and the treatment of GPR84-mediated disorders.
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公开(公告)号:US20210085626A1
公开(公告)日:2021-03-25
申请号:US17111146
申请日:2020-12-03
发明人: Lyne GAGNON , Pierre LAURIN
IPC分类号: A61K31/192 , A61P17/02 , A61P19/08 , A61K8/36 , A61K8/365 , A61Q19/08 , C07C57/30 , C07C57/32 , C07C57/58 , C07C59/52 , C07C59/84
摘要: Described herein are compounds of Formula I, or pharmaceutically acceptable salts thereof, or combinations thereof, as well as uses thereof. Such uses include promoting tissue self-repair or tissue regeneration of an organ, stimulating the generation of tissue growth, modulating (e.g., increasing) the level of a tissue-repair marker, treating physical injury in an organ, tissue or cell, promoting wound healing, as well as anti-aging applications. Corresponding compositions, methods, kits, and uses are also described. Formula I wherein A is C5 alkyl, C6 alkyl, C5 alkenyl, C6 alkenyl, C(O)—(CH2)n—CH3 or CH(OH)—(CH2)n—CH3 wherein n is 3 or 4; R1 is H, F of OH; R2 is H, F, OH, C5 alkyl, C6 alkyl, C5 alkenyl, C6 alkenyl, C(O)—(CH2)n—CH3 or CH(OH)—(CH2)n—CH3 wherein n is 3 or 4; R3 is H, F, OH, or CH2Ph; R4 is H, F or OH; Q is 1) (CH2), C(O)OH wherein m is 1 or 2 2) CH(CH3)C(O)OH, 3) C(CH3)2C(O)OH, 4) CH(F)—C(O)OH, 5) CF2—C(O)OH or 6) C(O)—C(O)OH.
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公开(公告)号:US20230091528A1
公开(公告)日:2023-03-23
申请号:US17649744
申请日:2022-02-02
发明人: Shaun ABBOTT , Mylène DeLESELEUC , Julien MARTEL , Elyse BOURQUE , Jeremy GREEN , Alexandre LARIVÉE , Jean-Benoît GIGUÈRE , Elodie LANDAGARAY , Claudio STURINO
IPC分类号: C07D405/12 , C07D405/14 , C07D491/052 , C07D409/14 , C07D407/12 , C07D319/12 , C07D413/06 , C07D413/14 , C07D405/06 , C07D498/04 , C07D471/04 , C07D401/12 , C07D401/14 , C07D413/12 , C07D417/12 , C07D403/06 , C07D213/69
摘要: The present invention provides compounds, compositions thereof, and methods of using the same for the inhibition of GPR84, and the treatment of GPR84-mediated disorders.
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公开(公告)号:US10925846B2
公开(公告)日:2021-02-23
申请号:US15516635
申请日:2015-10-08
发明人: Lyne Gagnon , Brigitte Grouix
IPC分类号: A61K31/192 , A61K31/20 , A61K31/13 , A61K31/275 , A61K31/662 , A61K38/16 , A61P19/08 , A61P19/10
摘要: The present invention concerns the use of compounds for preventing and/or treating osteoporosis, for stimulating bone formation, for stimulating the differentiation and mineralization of osteoblasts, or for inhibiting bone resorption in a subject. These novel uses have been found for compounds represented by Formula I and pharmaceutically acceptable salts thereof. wherein: R1 and R2 are independently equal to H, F or OH; A is (CH2)mCOOH, W(CH2)mCOOH, or Y—CH(COOH)—(CH2)p-CH3 when B is H; or B is (CH2)mCOOH, W(CH2)mCOOH, or Y—CH(COOH)—(CH2)p—CH3 when A is H; or A and B are covalently bonded to form a five (5), six (6), or seven (7)-membered cycloalkyl substituted with COOH; where: Y is O, S, HN or CH2; W is 0, S or NH; m is 0-2; and p is 3-7; D is CO(CH2)nCH3 or CHOH(CH2)nCH3 or O(CH2)nCH3 where n is 2-6; and E is H or F.
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公开(公告)号:US20200172462A1
公开(公告)日:2020-06-04
申请号:US16780316
申请日:2020-02-03
发明人: Boulos ZACHARIE , Shaun ABBOTT , Lyne GAGNON , Pierre LAURIN , Brigitte GROUIX
IPC分类号: C07C53/134 , C07C57/30 , C07C57/58 , A61K31/192 , C07C59/52
摘要: The present invention relates to compounds of: or a pharmaceutically acceptable salt thereof, whereinA is O5 alkyl, C6 alkyl, C5 alkenyl, C6 alkenyl, C(O)—(CH2)n—CH3 or CH(OH)—(CH2)n—CH3 wherein n is 3 or 4;R1 is H, F or OH;R2 is C5 alkyl, C6 alkyl, C5 alkenyl, C6 alkenyl, C(O)—(CH2)n—CH3 or CH(OH)—(CH2)n—CH3 wherein n is 3 or 4;R3 is H, F, OH or CH2Ph;R4 is H, F or OH;Q is 1) (CH2)mC(O)OH wherein m is 1 or 2, 2) CH(CH3)C(O)OH, 3) C(CH3)2C(O)OH, 4) CH(F)—C(O)OH, 5) CF2—C(O)OH, or 6) C(O)—C(O)OH; and compositions comprising the same and the method using the same for the prevention or treatment of various fibrotic diseases and conditions in subjects, including pulmonary fibrosis, liver fibrosis, skin fibrosis, renal fibrosis, pancreas fibrosis, systemic sclerosis, cardiac fibrosis or macular degeneration.
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