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公开(公告)号:US20220298186A1
公开(公告)日:2022-09-22
申请号:US17616748
申请日:2020-06-16
IPC分类号: C07F9/6558 , C07F9/59
摘要: The disclosure relates to compounds of Formula (I), which are formyl peptide 2 (FPR2) receptor agonists and/or formyl peptide 1 (FPR1) receptor agonists. The disclosure also provides compositions and methods of using the compounds, for example, for the treatment of atherosclerosis, heart failure, chronic obstructive pulmonary disease (COPD), and related diseases.
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公开(公告)号:US11447451B2
公开(公告)日:2022-09-20
申请号:US16878491
申请日:2020-05-19
申请人: AM Chemicals LLC
IPC分类号: C07D211/22 , C07F9/59 , C07F9/6561 , C07F9/6558 , C07F9/568 , C07F9/24 , C07D205/04 , C07D401/12 , C07D409/06 , C07D491/18 , C07D493/10 , C07D495/04 , C07H1/00 , C07H15/26 , C07H21/00 , C07J43/00
摘要: Novel non-nucleoside solid supports and phosphoramidite building blocks for preparation of synthetic oligonucleotides containing at least one non-nucleosidic moiety conjugated to a ligand of practical interest and synthetic processes for making the same are disclosed. Furthermore, oligomeric compounds are prepared using said solid supports and phosphoramidite building blocks, preferably followed by removal of protecting groups to provide oligonucleotides conjugated to ligands of interest.
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3.
公开(公告)号:US11214569B2
公开(公告)日:2022-01-04
申请号:US16700088
申请日:2019-12-02
发明人: Gerald Horn
IPC分类号: C07D453/02 , C07F9/59 , C07F9/6561 , C07D453/00 , A61P27/06 , A61K47/40
摘要: The present invention is directed to compounds of the formula and salts or esters thereof. The present invention is further directed to ophthalmological compositions comprising a therapeutically effective amount of a compound of the present invention and one or more pharmaceutically acceptable excipients. The present invention is further directed to a methods of treating presbyopia or glaucoma or reducing hyperemia comprising administering to a patient in need thereof a therapeutically effective amount of a compound of the present invention.
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公开(公告)号:US20210139897A1
公开(公告)日:2021-05-13
申请号:US16936906
申请日:2020-07-23
IPC分类号: C12N15/113 , C07F9/59 , C07F9/572 , C07F9/6558 , C07F9/6561 , C07F9/6584 , C07H21/00 , A61K31/496 , A61K31/5377 , C07D265/30 , C07D295/108 , C07F9/22 , C07F9/26 , C07F9/6544
摘要: Oligonucleotide analogues comprising modified intersubunit linkages and/or modified 3′ and/or 5′-end groups are provided. The disclosed compounds are useful for the treatment of diseases where inhibition of protein expression or correction of aberrant mRNA splice products produces beneficial therapeutic effects.
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公开(公告)号:US10851123B2
公开(公告)日:2020-12-01
申请号:US16078585
申请日:2017-02-22
发明人: Craig Husfeld , Andrei W. Konradi
IPC分类号: A61P29/00 , C07F9/09 , C07D233/64 , C07D207/16 , C07C259/06 , C07C271/48 , C07C271/54 , C07C275/42 , C07C279/14 , C07C305/10 , C07C307/02 , C07C307/10 , C07C323/12 , C07C323/44 , C07C323/60 , C07C233/20 , C07C233/27 , C07C233/51 , C07F9/12 , C07F9/24 , C07F9/59 , C07D211/26 , C07D213/81 , C07D211/28 , C07D295/185 , C07D207/09
摘要: Described herein are compounds, pharmaceutical compositions and medicaments that include such compounds, and methods of using such compounds to modulate transient receptor potential vanilloid 1 receptor (TRPV1) activity.
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公开(公告)号:US10787472B2
公开(公告)日:2020-09-29
申请号:US16283904
申请日:2019-02-25
发明人: Corey Anderson , Sara Sabina Hadida Ruah , Julian Marian Charles Golec , Beili Zhang , Benjamin Joseph Littler , Ali Keshavarz-Shokri , Tim Edward Alcacio , Daniel T. Belmont
IPC分类号: C07F9/58 , C07F9/59 , C07F9/576 , A61K31/675 , A61K45/06
摘要: The invention relates to prodrug compounds of formula I: wherein R2, R3, R5, R7 and X are as defined herein. The invention also provides pharmaceutically acceptable compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various disorders, including pain. The compounds of formula I possess advantageous solubility and physicochemical properties.
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公开(公告)号:US10392346B2
公开(公告)日:2019-08-27
申请号:US16035502
申请日:2018-07-13
IPC分类号: C07D213/74 , C07D213/80 , C07D401/12 , C07D239/47 , C07D413/12 , C07D405/12 , C07D453/02 , C07F9/6512 , C07H19/048 , C07H13/08 , C07H15/26 , C07F9/6558 , A61K31/44 , A61K31/506 , A61K31/675 , A61K31/5377 , A61K31/496 , A61K31/4545 , A61K31/4439 , A61K31/706 , A61K31/553 , A61K31/551 , A61K31/541 , C07F9/58 , C07F9/59 , A61K31/4412 , A61K31/7052 , A61K31/4375 , A61K31/635 , A61K45/06 , A61K31/444 , A61K31/505 , C07F9/6503
摘要: There are provided compounds of formula IIb, wherein: LG1 represents imidazolyl, chloro, or aryloxy; and Z1 represents a structural fragment of formula V: wherein R2 to R4, R5a, L and X1 to X3 have meanings given in the description, or a salt or protected derivative thereof, wherein said protected derivative is a compound in which the carboxyl moiety of R4 is protected as a C1-8 alkyl ester. The compounds have antiinflammatory activity, for example through inhibition of one or more of members of: the family of p38 mitogen-activated protein kinase enzymes; Syk kinase; and members of the Src family of tyrosine kinases) and have use in therapy, including in pharmaceutical combinations, especially in the treatment of inflammatory diseases, including inflammatory diseases of the lung, eye and intestines.
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公开(公告)号:US10376502B2
公开(公告)日:2019-08-13
申请号:US14813931
申请日:2015-07-30
发明人: Yanming Du , Xiaodong Xu , Hong Ye , Jinhong Chang , Timothy M. Block
IPC分类号: A61K31/45 , A61K31/4015 , C07F9/59 , C07D207/12 , C07D211/44 , C07D211/46 , C07D413/06
摘要: Pharmaceutical compositions of the invention comprise alkylated imino sugars derivatives having a disease-modifying action in the treatment of diseases associated with glucosidase activity that include Viral hemorrhagic fevers, and any other diseases involving glucosidase activity.
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公开(公告)号:US10329314B2
公开(公告)日:2019-06-25
申请号:US15908508
申请日:2018-02-28
申请人: CHEMOCENTRYX, INC.
发明人: Pingchen Fan , Antoni Krasinski , Venkat Reddy Mali , Shichang Miao , Sreenivas Punna , Yang Song , Valentino J. Stella , Yibin Zeng , Penglie Zhang
IPC分类号: C07D211/60 , A61K31/451 , A61K31/675 , A61K45/06 , C07F9/6558 , C07F9/59 , A61K31/496
摘要: Compounds are provided to modulate the C5a receptor. The compounds have the following Formula (I): including stereoisomers and pharmaceutically acceptable salts thereof, wherein R1, R2 and R3 are as defined herein. Methods associated with preparation and use of such compounds, as well as pharmaceutical compositions comprising such compounds, are also disclosed.
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公开(公告)号:US20190127733A1
公开(公告)日:2019-05-02
申请号:US15766578
申请日:2016-10-07
发明人: David Charles Donnell Butler , Sethumadhavan Divakaramenon , Christopher J. Francis , Maria David Frank-Kamenetsky , Naoki Iwamoto , Genliang Lu , Subramanian Marappan , Meena . , Chandra Vargeese , Gregory L. Verdine , Hailin Yang , Jason Jingxin Zhang
摘要: Among other things, the present disclosure relates to designed oligonucleotides, compositions, and methods thereof. In some embodiments, provided oligonucleotide compositions provide altered splicing of a transcript. In some embodiments, provided oligonucleotide compositions have low toxicity. In some embodiments, provided oligonucleotide compositions provide improved protein binding profiles. In some embodiments, provided oligonucleotide compositions have improved delivery. In some embodiments, provided oligonucleotide compositions have improved uptake. In some embodiments, the present disclosure provides methods for treatment of diseases using provided oligonucleotide compositions.
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