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公开(公告)号：US20220411468A1
公开(公告)日：2022-12-29
申请号：US17377338
申请日：2021-07-15
发明人： Alexander Alanine , Julien Beignet , Konrad Bleicher , Bernhard Fasching , Hans Hilpert , Taishan Hu , Dwight MacDonald , Stephen Jackson , Sabine Kolczewski , Carsten Kroll , Adrian Schaeublin , Hong Shen , Theodor Stoll , Helmut Thomas , Amal Wahhab , Claudia Zampaloni
摘要： The present invention provides compounds of formula (I) wherein X1 to X8 and R1 to R8 are as described herein, as well as pharmaceutically acceptable salts thereof. Further the present invention is concerned with the manufacture of the compounds of formula (I), pharmaceutical compositions comprising them and their use as medicaments for the treatment of diseases and infections caused by Acinetobacter baumannii.
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公开(公告)号：US20220409709A1
公开(公告)日：2022-12-29
申请号：US17309648
申请日：2019-12-13
摘要： Antigenic compositions comprising one or more labyrinthin-derived peptides are described herein. In some embodiment, each peptide of the antigenic composition comprises a T-cell epitope and/or a B-cell epitope. In other aspects, the present disclosure provides, e.g., vaccine compositions comprising tin antigenic composition disclosed herein, including kits, medicines, and compositions (such as pharmaceutical compositions and unit dosages) thereof. Also provided are methods of using the compositions disclosed herein, such as methods of treatment thereof and methods of producing antibodies, and antibody compositions thereof, against the one or more labyrinthin-derived peptides or a portion thereof.
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13.发明申请公开(公告)号：US20220388984A1
公开(公告)日：2022-12-08
申请号：US17359424
申请日：2021-06-25
发明人： Andrew P. Crew , Hanqing Dong , Keith R. Hornberger , Yimin Quian , Jing Wang
IPC分类号： C07D401/14 , A61K47/54 , A61P15/00 , A61P35/00 , A61K31/454 , A61K31/4545 , A61K31/4725 , A61K31/496 , A61K31/497 , A61K31/501 , A61K31/519 , A61K31/5386 , A61K31/551 , A61K38/05 , A61K38/06 , A61K45/06 , C07D401/04 , C07D471/04 , C07D471/10 , C07D487/04 , C07D487/08 , C07D487/10 , C07D498/10 , C07K5/078 , C07K5/083
摘要： The present disclosure relates to bifunctional compounds, which find utility as modulators of estrogen receptor (target protein). In particular, the present disclosure is directed to bifunctional compounds, which contain on one end at least one of a Von Hippel-Lindau ligand, a cereblon ligand, Inhibitors of Apoptosis Proteins ligand, mouse double-minute homolog 2 ligand, or a combination thereof, which binds to the respective E3 ubiquitin ligase, and on the other end a moiety which binds the target protein, such that the target protein is placed in proximity to the ubiquitin ligase to effect degradation (and inhibition) of target protein. The present disclosure exhibits a broad range of pharmacological activities associated with degradation/inhibition of target protein. Diseases or disorders that result from aggregation or accumulation of the target protein are treated or prevented with compounds and compositions of the present disclosure.
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公开(公告)号：US20220332758A1
公开(公告)日：2022-10-20
申请号：US17642499
申请日：2020-09-11
发明人： Pawel A. OSMULSKI , Maria Gaczynska , Andrew Pickering , Przemyslaw Karpowicz , Elzbieta Jankowska
摘要： Disclosed herein, are peptides capable of activating proteasome activity, and pharmaceutical compositions containing the peptides and methods treating Alzheimer's disease. Disclosed herein are compositions comprising: A) a peptide, wherein the peptide comprises the amino acid sequence GRKKR-RQ-AibG-RPS (SEQ ID NO: 4), or a fragment or variant thereof, B) a peptide, wherein the peptide comprises the amino acid sequence GRKKRRQ-AibG-QR-RKKRG (SEQ ID NO: 5), or a fragment or variant thereof, or C) a peptide, wherein the peptide comprises the amino acid sequence KKK/KKK-DABA-K KK (SEQ ID NO: 6) or a fragment or variant thereof.
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公开(公告)号：US20220315624A1
公开(公告)日：2022-10-06
申请号：US17610778
申请日：2020-05-13
申请人： YALE UNIVERSITY
发明人： Jonathan Ellman , Ryan Scamp , Scott Miller , Edward de Ramon
摘要： Provided herein are thiostrepton analogues, such as but not limited to compounds of Formula I, with improved aqueous solubility and antibacterial properties against antibiotic-resistant bacterial strains. The methods of the disclosure further provide a chemoselective way to introduce diverse functionality into peptides or protein comprising a dehydroalanine residue.
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公开(公告)号：US20220211797A1
公开(公告)日：2022-07-07
申请号：US17392724
申请日：2021-08-03
申请人： GENENTECH, INC.
摘要： Novel inhibitors of IAP that are useful as therapeutic agents for treating malignancies and have the general formula I: wherein R1, R2, R3, R4, R5 and R6 are as described herein.
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公开(公告)号：US11345724B2
公开(公告)日：2022-05-31
申请号：US16305693
申请日：2017-06-06
发明人： Ashwin Chari , Holger Stark , Jil Schrader , Fabian Henneberg
摘要： The present invention relates to a compound of formula (I), wherein X is C═O, C═S or B—OH; Y is an electrophile and Z is a leaving group, or Y═Z is an electrophile; R1 comprises or consists of (a) (i) a first group binding to a proteolytic site of a proteasome, the first group being bound to X; and (ii) optionally a second group enhancing delivery; or (b) a group binding between subunits β1 and β2 of a proteasome; R2 and R3 are independently selected from H, methyl, methoxy, ethyl, ethenyl, ethynyl and cyano, wherein methyl and ethyl may be substituted with OH or halogen.
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公开(公告)号：US20220089639A1
公开(公告)日：2022-03-24
申请号：US17228284
申请日：2021-04-12
申请人： Novartis AG
IPC分类号： C07K5/103 , C07K5/083 , C07K5/062 , A61K49/00 , C07C271/22 , C07C317/28 , C07K1/13 , C07K5/072 , A61K47/64 , C07D229/02 , C07D257/08 , C07D209/42 , C07K7/02
摘要： The present invention relates to methods and reagents for use in site-selective modification of proteins having lysine residues with functionalized peptides using a chemoenzymatic microbial transglutaminase-mediated reaction. The functionalized proteins may be used for study or therapeutic uses.
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公开(公告)号：US11246763B2
公开(公告)日：2022-02-15
申请号：US15890217
申请日：2018-02-06
IPC分类号： A61F13/02 , A61F13/00 , B82Y5/00 , C07K5/062 , C07K5/072 , C07K5/083 , C07K5/103 , C07K7/02 , C07K9/00 , G01N33/574 , A61K47/64 , A61K47/66 , A61K38/00
摘要： Devices, bandages, kits and methods are described that can control or regulate the mechanical environment of a wound to ameliorate scar and/or keloid formation. The mechanical environment of a wound includes stress, strain, and any combination of stress and strain. The control of a wound's mechanical environment can be active, passive, dynamic, or static. The devices are configured to be removably secured to a skin surface in proximity to the wound site and shield the wound from endogenous and/or exogenous stress.
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公开(公告)号：US20220017572A1
公开(公告)日：2022-01-20
申请号：US17374437
申请日：2021-07-13
IPC分类号： C07K5/103 , C07K5/083 , A61P31/14 , A61K38/08 , C07K5/09 , C07K7/06 , C07K5/072 , C07K7/08 , A61K38/05 , C07K5/113 , A61K38/07 , A61K38/00
摘要： Disclosed are geminoid peptide-like compound according to Formula I: R1—C(═O)—Zn—NR3-R2 (I) in which R1 and R2 are each independently saturated, partly saturated or unsaturated, straight, branched or cyclic alkyl chains, wherein R1 has a number of C atoms of 11 or more, preferably 11 to 19, and R2 has a number of C atoms of 12 or more, preferably 12 to 20; R3 is hydrogen or C1-C6 alkyl; n is an integer from 1-15; each Z independently is an amino acid residue, wherein Zn comprises an N-terminus attached to C(═O) and a C-terminus that is attached to NR3, for use as a medicament.
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