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公开(公告)号:US10806794B2
公开(公告)日:2020-10-20
申请号:US16107689
申请日:2018-08-21
申请人: Nektar Therapeutics
IPC分类号: A61K31/655 , A61K31/34 , A61K47/55 , A61K31/4402 , A61K31/4433 , A61K31/635 , A61K38/05 , A61K47/60
摘要: Provided herein (among other things) are protease inhibitor compounds having enhanced features, along with methods for administering such compounds. For example, the subject compounds can be administered without concomitant administration of a CYP3A4 inhibitor, have increased therapeutic index and/or increased potency, and are low-resistance inducing in nature.
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公开(公告)号:US20200282002A1
公开(公告)日:2020-09-10
申请号:US16783481
申请日:2020-02-06
申请人: Medivir AB
IPC分类号: A61K38/05 , C07D403/06 , C07K5/062 , A61K38/07 , A61K45/06 , C07D403/14 , C07K5/02 , A61K31/404 , A61N5/06 , A61N5/10 , C07K5/06 , C12N5/09 , A61K31/555
摘要: A SMAC mimetic and pharmaceutical compositions thereof and methods of use.
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公开(公告)号:US20200268828A1
公开(公告)日:2020-08-27
申请号:US16797211
申请日:2020-02-21
发明人: Hiroshi INOUE , Kumi KIMURA , Nobuhiko TACHIBANA
摘要: A peptide having an effect of suppressing hepatic lipogenesis, where a peptide is one or two or more peptides selected from 11 dipeptides (Ala-Gly, His-Asn, His-Ser, His-Thr, His-Trp, Val-Met, Trp-Glu, Trp-Lys, Tyr-Lys, Tyr-Ser and Tyr-Tyr) and 25 tripeptides (Val-Ile-Leu, Gly-Ser-Leu, Val-Leu-Gln, His-Ala-Gln, Arg-Ala-Val, Lys-Leu-Gly, Ile-Val-Ile, Lys-Pro-Ile, Leu-Val-Ile, Leu-Arg-Asp, Gln-Glu-Glu, Ser-Gly-Glu, Arg-Trp-Phe, Asp-Phe-Phe, Asp-Val-Phe, Pro-Phe-Tyr, Phe-Ile-Arg, Asn-Gly-Arg, Ile-Ile-Pro, Ile-Asp-Arg, Ile-His-Arg, Ile-Asp-Arg, Asn-Arg-Val, Ser-Ser-Val and Val-Phe-Val), is provided. The peptide may be used to a food composition for suppressing hepatic lipogenesis and an agent for suppressing hepatic lipogenesis.
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公开(公告)号:US10730862B2
公开(公告)日:2020-08-04
申请号:US14371956
申请日:2013-01-11
申请人: YALE UNIVERSITY , GLAXOSMITHKLINE INTELLECTUAL PROPERTY DEVELOPMENT LIMITED , CAMBRIDGE ENTERPRISE LIMITED UNIVERSITY OF CAMBRIDGE
发明人: Craig M. Crews , Dennis Buckley , Alessio Ciulli , William Jorgensen , Peter C. Gareiss , Inge Van Molle , Jeffrey Gustafson , Hyun-Seop Tae , Julien Michel , Denton Wade Hoyer , Anke G. Roth , John David Harling , Ian Edward David Smith , Afjal Hussain Miah , Sebastien Andre Campos , Joelle Le
IPC分类号: C07D413/14 , C07D417/12 , C07D417/14 , C07D401/06 , C07D401/10 , C07D403/06 , C07D405/06 , C07D405/12 , C07D207/16 , C07D413/12 , C07D207/26 , C12N9/00 , A61K47/54 , A61K47/64 , A61K47/55 , A61K31/422 , A61K31/427 , A61K31/437 , A61K31/4439 , A61K31/454 , A61K31/5377 , A61K38/05 , A61K38/06 , A61K45/06 , C07D413/06 , C07D471/04 , C07J43/00
摘要: The present invention relates to bifunctional compounds, which find utility as modulators of targeted ubiquitination, especially inhibitors of a variety of polypeptides and other proteins that are degraded and/or otherwise inhibited by bifunctional compounds of the present invention. In particular, the present invention is directed to compounds, which contain on one end a VHL ligand that binds to the ubiquitin ligase and on the other end a moiety that binds a target protein, such that the target protein is placed in proximity to the ubiquitin ligase to effect degradation (and inhibition) of that protein. The present invention exhibits a broad range of pharmacological activities associated with compounds of the present invention, consistent with the degradation/inhibition of targeted polypeptides.
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公开(公告)号:US20200237791A1
公开(公告)日:2020-07-30
申请号:US16785498
申请日:2020-02-07
申请人: Bruce W. Kneller
发明人: Bruce W. Kneller
IPC分类号: A61K31/7016 , A61K9/00 , A61K38/05 , A61K33/00 , A61K31/197 , A61K31/7076 , A61K31/70 , A61K45/06 , A61K31/566 , A61K31/122
摘要: The present invention is directed to a dietary supplement comprising palatinose or a derivative thereof. The dietary supplement may be a nutritional product, a sports performance product, a weight loss product or a meal replacement product. The present invention is also directed to a method of increasing the absorption of a compound into the bloodstream, cells and tissue comprising administering palatinose, or a derivative thereof, in combination with the compound. The present invention also relates to a diluent for parenteral compounds. The diluent comprises palatinose or a derivative thereof. Another aspect of the present invention is directed to a method of decreasing the recovery time to pre-performance levels of total adenosine triphosphate (ATP) levels in a mammal comprising administering palatinose, or a derivative thereof, to the mammal. The present invention is further directed to a method of supplying a compound to a diabetic patient, burn victim patient or trauma victim patient. The method comprises administering palatinose, or a derivative thereof, in combination with the compound.
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公开(公告)号:US20200237637A1
公开(公告)日:2020-07-30
申请号:US16845513
申请日:2020-04-10
发明人: Ruey J. Yu , Eugene J. Van Scott
IPC分类号: A61K8/64 , A61Q19/06 , A61K9/00 , C07K5/06 , C07K5/078 , C07K5/065 , C07K5/062 , A61Q19/08 , A61Q19/00 , A61K38/05 , C07K5/072 , C07K5/02 , A61K8/67 , A61K31/07
摘要: Methods of treating aging related skin changes and of increasing skin thickness with topical administration of N-acyldipeptide derivatives are described. Compositions comprising N-acyldipeptide derivatives, are therapeutically effective for increasing skin thickness, and for treating extrinsic and intrinsic aging and aging related skin changes, such as fine lines, wrinkles, photoaging, hyperpigmentation, laxity, age spots, lentigines, mottled skin, and cellulite.
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公开(公告)号:US10653604B2
公开(公告)日:2020-05-19
申请号:US16022809
申请日:2018-06-29
发明人: Ruey J. Yu , Eugene J. Van Scott
IPC分类号: A61K8/64 , C07K5/02 , C07K5/062 , C07K5/078 , C07K5/072 , A61K31/07 , A61K8/67 , A61K38/05 , A61Q19/00 , A61Q19/08 , C07K5/065 , C07K5/06 , A61K9/00 , A61Q19/06 , A61Q5/00 , A61Q19/02
摘要: Methods of treating aging related skin changes and of increasing skin thickness with topical administration of N-acyldipeptide derivatives and retinol are described. Combinations of retinol and N-acyldipeptide derivatives, are therapeutically effective for increasing skin thickness, and for treating extrinsic and intrinsic aging and aging related skin changes, such as fine lines, wrinkles, photoaging, hyperpigmentation, laxity, age spots, lentigines, mottled skin, and cellulite.
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公开(公告)号:US10568868B2
公开(公告)日:2020-02-25
申请号:US15885147
申请日:2018-01-31
发明人: Barbara Slusher , Jonathan Powell
IPC分类号: A61K31/223 , A61K31/4045 , A61K38/05 , A61K31/655 , A61K39/395 , A61K31/22 , A61K31/225
摘要: The disclosure provides methods of treating a condition, disease, or disorder in a subject that involves metabolically reprogrammed cells whose activation, function, growth, proliferation, or survival depends on increased activity of at least one metabolic pathway selected from the group consisting of glutamine metabolism, glycolysis, and fatty acid synthesis, comprising administering to the subject a compound having formula (I): and the pharmaceutically acceptable salts thereof, wherein R1, R2, R2′, and X are as defined as set forth in the specification. Compounds having formula (I) are prodrugs that release glutamine analogs, e.g., 6-diazo-5-oxo-L-norleucine (DON).
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公开(公告)号:US10538500B2
公开(公告)日:2020-01-21
申请号:US16059960
申请日:2018-08-09
发明人: Martin Johansson , Olov Sterner
IPC分类号: C07D307/93 , A61K31/365 , A61K38/05 , A61K38/06 , C07K5/02 , C07K5/062
摘要: Prodrugs of galiellactone, and derivatives thereof, are provided by reacting the parent compound, e.g. galiellactone, with a thiol. Such drugs may be administered orally to treat cancer and other proliferative diseases.
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公开(公告)号:US10532018B2
公开(公告)日:2020-01-14
申请号:US16305492
申请日:2017-06-29
申请人: ANPEP INC.
发明人: Sang Moon Kang , Seock Yeon Hwang , Mi Hye Lim , Chung Park , Eun Jin Shin , Kee-young Lee , Un Kyu Park , Hyun Ji Lim , Dong Hyun Yang , Sang Joo Cha
摘要: A skin whitening method including: administering to a subject a cosmetic composition including a tranexamic acid-peptide having skin whitening activity selected from the group consisting of Tranexamil-AS, Tranexamil-AT, Tranexamil-AP, Tranexamil-GP, Tranexamil-ES, Tranexamil-KK, Tranexamil-HK, Tranexamil-MY, Tranexamil-GH, Tranexamil-MA, Tranexamil-AH, Tranexamil-CC, Tranexamil-SA, Tranexamil-WA, Tranexamil-WE, Tranexamil-KD, Tranexamil-NA, Tranexamil-TS, Tranexamil-SS, Tranexamil-EC, Tranexamil-TA, Tranexamil-PF, Tranexamil-VS, Tranexamil-VV, Tranexamil-VP, Tranexamil-AA, Tranexamil-PS, Tranexamil-HA, Tranexamil-GK, Tranexamil-KV, Tranexamil-AR, Tranexamil-RP, Tranexamil-PQ, Tranexamil-QG, Tranexamil-PP, Tranexamil-VR, Tranexamil-SV, Tranexamil-ET, Tranexamil-CG and Tranexamil-NT.
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