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1.发明公开公开(公告)号：US20240254103A9
公开(公告)日：2024-08-01
申请号：US17914153
申请日：2021-03-12
发明人： Ge Hyeong LEE , Jee Yeon SEO , Jeong Heon YU , In Hae YE , Ho Chul SHIN , Jee Hee SUH , Seong Hwan KIM , Jin Sook SONG , Seong Hyeon SIM , Chong Hak CHAE , Hee Yeon KANG , Ji Hun LEE , Keon Ha HWANG
IPC分类号： C07D401/14 , C07D403/04 , C07D405/14 , C07D413/14 , C07D471/04 , C07D487/04 , C07D491/107 , C07D491/18
CPC分类号： C07D401/14 , C07D403/04 , C07D405/14 , C07D413/14 , C07D471/04 , C07D487/04 , C07D491/107 , C07D491/18
摘要： The present invention relates to a novel pyrimidine derivative, and a composition for preventing or treating neurodegenerative diseases and cancer, comprising same, the pyrimidine derivative having a LRRK2 protein inhibitory activity, and effectively passing through a blood-brain barrier (BBB) so as to be effectively used as a pharmaceutical composition for preventing or treating neurodegenerative diseases and cancer.
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公开(公告)号：US11987590B2
公开(公告)日：2024-05-21
申请号：US17345570
申请日：2021-06-11
发明人： Gregory Lawrence Verdine , Brian Roger Bowman , Mathew Edward Sowa , Joshua Alan Van Dyke Blodgett , Keith Earl Robison , Dylan Talbot Stiles , Jay Paul Morgenstern , Sharon Ann Townson , Uddhav Kumar Shigdel
IPC分类号： A61K31/407 , A61K31/4353 , A61K31/436 , A61K47/62 , A61K47/64 , A61P35/00 , C07D491/18 , C07D498/18 , C12N9/90 , C12P17/18 , A61K38/00
CPC分类号： C07D491/18 , A61K31/407 , A61K31/4353 , A61K31/436 , A61K47/62 , A61K47/64 , A61P35/00 , C07D498/18 , C12N9/90 , C12P17/18 , C12Y502/01008 , A61K38/00
摘要： The invention features compounds (e.g., macrocyclic compounds) capable of modulating biological processes, for example through binding to a presenter protein (e.g., a member of the FKBP family, a member of the cyclophilin family, or PIN1) and a target protein such as CEP250. These compounds bind endogenous intracellular presenter proteins, such as the FKBPs or cyclophilins, and the resulting binary complexes selectively bind and modulate the activity of the target protein. Formation of a tripartite complex among the presenter protein, the compound, and the target protein is driven by both protein-compound and protein-protein interactions, and both are required for modulation of target protein activity.
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公开(公告)号：US20230212152A1
公开(公告)日：2023-07-06
申请号：US18008914
申请日：2021-06-09
发明人： Lee D. Arnold , Andy Jennings , Walter Keung
IPC分类号： C07D403/12 , C07D207/267 , C07D417/14 , C07D209/42 , C07D471/04 , C07D405/14 , C07D403/14 , C07D401/14 , C07D471/10 , C07D401/12 , C07D417/12 , C07D487/10 , C07D209/52 , C07D209/44 , C07D209/56 , C07D413/14 , C07D491/107 , C07D513/04 , C07D491/18 , C07F7/08 , C07D207/34 , C07D221/20 , C07D209/54 , A61P31/14 , A61K47/64 , A61K45/06 , C12N9/50
CPC分类号： C07D403/12 , C07D207/267 , C07D417/14 , C07D209/42 , C07D471/04 , C07D405/14 , C07D403/14 , C07D401/14 , C07D471/10 , C07D401/12 , C07D417/12 , C07D487/10 , C07D209/52 , C07D209/44 , C07D209/56 , C07D413/14 , C07D491/107 , C07D513/04 , C07D491/18 , C07F7/0812 , C07F7/0816 , C07D207/34 , C07D221/20 , C07D209/54 , A61P31/14 , A61K47/64 , A61K45/06 , C12N9/506 , C12Y304/22066
摘要： The disclosure provides compounds of formula II with warheads and their use in treating medical diseases or disorders, such as viral infections. Pharmaceutical compositions and methods of making various compounds with warheads are provided. The compounds are contemplated to inhibit proteases, such as the 3C, CL- or 3CL-like protease.
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公开(公告)号：US20230183261A1
公开(公告)日：2023-06-15
申请号：US17649906
申请日：2022-02-03
发明人： Andrew S. Judd , Aaron R. Kunzer , Chunqiu Lai , Andrew J. Souers , Gerard M. Sullivan , Zhi-Fu Tao , Jesse A. Teske , Anthony Mastracchio , Xilu Wang , Cheng Ji , Michael D. Wendt , Xiaohong Song , George A. Doherty , Katja Jantos , Wilfried Braje , Andreas Kling , Frauke Pohlki , Thomas D. Penning
IPC分类号： C07D495/16 , C07D495/18 , A61K45/06 , C07D495/22 , C07D491/18 , A61K31/519 , C07D491/22 , A61P35/00 , A61P35/02
CPC分类号： C07D495/16 , C07D495/18 , A61K45/06 , C07D495/22 , C07D491/18 , A61K31/519 , C07D491/22 , A61P35/00 , A61P35/02
摘要： The present disclosure provides for compounds of formula (I)
wherein A2, A3, A4, A6, A7, A8, A15, RA, R5, R9, R10A, R10B, R11, R12, R13, R14, R16, W, X, and Y have any of the values defined in the specification, and pharmaceutically acceptable salts thereof, that are useful as agents in the treatment of diseases and conditions, including cancer. Also provided are pharmaceutical compositions comprising compounds of formula (I).-
公开(公告)号：US20230159458A1
公开(公告)日：2023-05-25
申请号：US17817267
申请日：2022-08-03
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
CPC分类号： C07D211/22 , C07F9/59 , C07F9/6561 , C07F9/65583 , C07F9/65586 , C07F9/568 , C07F9/2458 , C07D205/04 , C07D401/12 , C07D409/06 , C07D491/18 , C07D493/10 , C07D495/04 , C07H1/00 , C07H15/26 , C07H21/00 , C07J43/003 , Y02P20/55
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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公开(公告)号：US20170334923A1
公开(公告)日：2017-11-23
申请号：US15528339
申请日：2015-11-25
IPC分类号： C07D491/18 , A61K31/485 , A61K9/70 , A61K9/00 , A61K47/38
CPC分类号： C07D491/18 , A61K9/0002 , A61K9/0073 , A61K9/7092 , A61K31/485 , A61K47/38 , A61P25/04 , A61P25/24 , C07D471/18 , C07D495/18
摘要： The present invention provides a compound having the structure wherein A is a ring structure, with or without substitution; X1 is C or N; X2 is N, O, or S; Y1 is H, -(alkyi), -(alkenyl), -(alkynyl), -(cycloalkyi), (haloalkyi), -(alkyl)-O-(alkyl) or -(alkyl)-(cycloalkyl); Y 2 is H, -(alkyi), -(alkenyl), -(alkynyl), -(cycloalkyi), (haloalkyi), -(alkyl)-O-(alkyl) or -(alkyl)-(cycloalkyl); Y3 is H-(alkyi), -(alkenyl), -(alkynyl), -(cycloalkyi), (haloalkyi), -(alkyl)-O-(alkyl) or -(alkyl)-(cycloalkyl); Y 4 is H-(alkyi), -(alkenyl), -(alkynyl), -(cycloalkyi), (haloalkyi), -(alkyl)-O-(alkyl) or -(alkyl)-(cycloalkyl); Y5 is H, -(alkyi), -(alkenyl), -(alkynyl), -(cycloalkyi), (haloalkyi), -(alkyl)-O-(alkyl) or -(alkyl)-(cycloalkyl); a and P are each present or absent and when present each is a bond.
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公开(公告)号：US20170313720A1
公开(公告)日：2017-11-02
申请号：US15498788
申请日：2017-04-27
发明人： Snezna ROGELJ , Liliya FROLOVA , Alexander KORNIENKO , Sean HENRY
IPC分类号： C07D495/18 , C07D491/18 , C07D471/08
CPC分类号： C07D495/18 , C07D471/08 , C07D491/18
摘要： The present disclosure describes a method to treat conditions, including cancer, using compounds that can target resistant cancer cells. The compounds of the invention can decrease the rate of proliferation of drug-resistant cancer cells, such as glioma, lung cancer, and uterine sarcoma.
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8.发明申请公开(公告)号：US20170253606A1
公开(公告)日：2017-09-07
申请号：US15315226
申请日：2015-06-03
发明人： Wu ZHONG , Song LI , Shuang CAO , Ruiyuan CAO , Junhai XIAO , Xinbo ZHOU , Xingzhou LI
IPC分类号： C07D491/18 , A61L31/16 , A61L31/08
CPC分类号： C07D491/18 , A61K31/395 , A61L31/08 , A61L31/16 , A61L2300/426
摘要： The present invention pertains to the field of pharmaceutical chemicals, and relates to a rapamycin derivative of Formula I, and a preparation method, pharmaceutical composition and use thereof. The compounds of the present invention overcome the defects of rapamycin in terms of water solubility and metabolic properties, and some of the compounds have an in vitro anti-tumor activity superior to rapamycin, have less toxicity to normal cells than rapamycin, and have very good druggability.
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9.发明申请公开(公告)号：US20170226122A1
公开(公告)日：2017-08-10
申请号：US15492180
申请日：2017-04-20
发明人： Rudi Fasan , Kai-Dong Zhang
IPC分类号： C07D493/18 , C12P17/18 , C12N9/02
CPC分类号： C07D493/18 , C07D491/18 , C12N9/0042 , C12N9/0071 , C12P17/181 , C12Y106/02004 , C12Y114/00
摘要： Derivatives of the antimalarial agent artemisinin, compositions comprising the derivatives, methods for preparing the derivatives, and their uses in pharmaceutical compositions intended for the treatment of parasitic infections are provided. Methods are provided for the production of artemisinin derivatives via functionalization of positions C7 and C6a, and optionally, in conjunction with modifications at positions C10 and C9, via chemoenzymatic methods. Recombinant cytochrome P450 polypeptides are also provided for use in the methods. The artemisinin derivatives can be used for the treatment of malaria and other parasitic infections, alone or in combination with other antiparasitic drugs.
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公开(公告)号：US20170197983A1
公开(公告)日：2017-07-13
申请号：US15467548
申请日：2017-03-23
发明人： Tatsuki KOIKE , Yuichi KAJITA , Masato YOSHIKAWA , Shuhei IKEDA , Eiji KIMURA , Tomoaki HASUI , Toshiya NISHI , Hiromi FUKUDA
IPC分类号： C07D498/08 , C07D413/14 , C07D417/14 , C07D471/08 , C07D471/10 , C07D405/14 , C07D213/74 , C07D239/42 , C07D401/04 , C07D401/14 , C07D487/18
CPC分类号： C07D498/08 , A61K9/2018 , A61K9/4858 , C07D213/12 , C07D213/72 , C07D213/74 , C07D239/42 , C07D401/04 , C07D401/12 , C07D401/14 , C07D403/04 , C07D403/12 , C07D403/14 , C07D405/12 , C07D405/14 , C07D413/04 , C07D413/14 , C07D417/04 , C07D417/14 , C07D451/02 , C07D451/04 , C07D471/08 , C07D471/10 , C07D487/08 , C07D487/10 , C07D487/18 , C07D491/08 , C07D491/18 , C12N9/99
摘要： An object of the present invention is to provide a compound having a superior CH24H inhibitory action, which is useful as an agent for the prophylaxis or treatment of epilepsy, neurodegenerative disease and the like. The present invention relates to a compound represented by the formula: wherein each symbol is as defined in the specification, or a salt thereof.
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