公开(公告)号：US12122852B2

公开(公告)日：2024-10-22

申请号：US18076033

申请日：2022-12-06

申请人： Creighton University ,  The Board of Regents of the University of Nebraska

发明人： Laura Hansen ,  Sandor Lovas ,  Nicholas Palermo

IPC分类号： C07K7/08 ,  A61K9/06 ,  A61K9/107 ,  A61K38/00 ,  A61P35/00 ,  C07K5/117

CPC分类号： C07K5/1024 ,  A61K9/06 ,  A61K9/107 ,  A61P35/00 ,  C07K7/08 ,  A61K38/00

摘要： Systems and methods for treatment of squamous cell carcinoma or other cancer utilizing targeting peptides are described. The targeting peptides interact with SCC cells or other cancerous cells to block or interfere with 14-3-3ε heterodimerization or CDC25A binding to 14-3-3ε. A peptide composition embodiment includes, but is not limited to, at least one of a first targeting peptide comprising a structure of Trp-Tyr-Trp-Lys-NH2 (SEQ ID NO: 1), a second targeting peptide comprising a structure of phospho-Ser178; Ac-Thr-Gln-Arg-Gln-Asn-Ser-(PO32−)-Ala-Pro-Arg-Met-Leu-Ser-Ser-Asn-NH2 (SEQ ID NO: 2), and a third targeting peptide comprising a structure of phospho-Thr507 residue; Ac-Arg-Thr-Lys-Ser-Arg-Thr(PO32−)-Trp-Ala-Gly-Glu-Lys-Ser-Lys-Arg-NH2 (SEQ ID NO: 3).

公开(公告)号：US12102705B2

公开(公告)日：2024-10-01

申请号：US15734033

申请日：2019-06-11

申请人： AZIENDE CHIMICHE RIUNITE ANGELINI FRANCESCO—A.C.R.A.F. S.p.A.

发明人： Francesca Mancini ,  Isabel Devesa Giner ,  Antonio Ferrer Montiel ,  Gregorio Fernandez Ballester ,  Giorgina Mangano ,  Cristina Bartella

IPC分类号： A61K8/64 ,  A61K38/00 ,  A61Q15/00 ,  C07K5/117 ,  C07K7/06 ,  C07K7/08

CPC分类号： A61K8/64 ,  A61Q15/00 ,  C07K5/1024 ,  C07K7/06 ,  C07K7/08 ,  A61K38/00

摘要： Peptides able to inhibit the muscarinic receptor M3 activity and to products comprising such peptides, in particular pharmaceutical and cosmetic products useful for ameliorating skin conditions mediated by the muscarinic receptor M3 activity, such as excessive perspiration, inflammation, sebum production, and cell adhesion, motility, growth, differentiation and proliferation.

公开(公告)号：US20240247030A1

公开(公告)日：2024-07-25

申请号：US18509211

申请日：2023-11-14

申请人： Seagen Inc.

发明人： Patrick J. BURKE ,  Scott JEFFREY ,  Joseph Z. HAMILTON

IPC分类号： C07K7/06 ,  A61K45/06 ,  A61K47/54 ,  A61K47/64 ,  A61K47/68 ,  C07H15/26 ,  C07K5/117 ,  C07K7/02 ,  C07K16/28

CPC分类号： C07K7/06 ,  A61K45/06 ,  A61K47/545 ,  A61K47/6415 ,  A61K47/6817 ,  A61K47/6849 ,  A61K47/6889 ,  C07H15/26 ,  C07K5/1024 ,  C07K7/02 ,  C07K16/2875 ,  C07K16/2878 ,  C07K16/2881 ,  C07K2317/24

摘要： Compounds and compositions are disclosed in which a quaternized drug unit is linked to a targeting ligand unit from which a tertiary amine-containing drug is released at the targeted site of action.
Methods for treating diseases characterized by the targeted abnormal cells, such as cancer or an autoimmune disease using the compounds and compositions of the invention are also disclosed.

公开(公告)号：US20190211058A1

公开(公告)日：2019-07-11

申请号：US16351669

申请日：2019-03-13

申请人： Onyx Therapeutics, Inc.

发明人： Mark S. Smyth ,  Guy J. Laidig

IPC分类号： C07K5/107 ,  C07K5/08 ,  C07K5/117 ,  A61K38/07 ,  C07K5/103 ,  C07K5/087

CPC分类号： C07K5/1016 ,  A61K38/00 ,  A61K38/07 ,  C07K5/0812 ,  C07K5/0827 ,  C07K5/1008 ,  C07K5/1024

摘要： Peptide-based compounds including heteroatom-containing, three-membered rings efficiently and selectively inhibit specific activities of N-terminal nucleophile (Ntn) hydrolases. The activities of those Ntn having multiple activities can be differentially inhibited by the compounds described. For example, the chymotrypsin-like activity of the 20S proteasome may be selectively inhibited with the inventive compounds. The peptide-based compounds include an epoxide or aziridine, and functionalization at the N-terminus. Among other therapeutic utilities, the peptide-based compounds are expected to display anti-inflammatory properties and inhibition of cell proliferation.

公开(公告)号：US20180170962A1

公开(公告)日：2018-06-21

申请号：US15895120

申请日：2018-02-13

申请人： Onyx Therapeutics, Inc.

发明人： Mark S. Smyth ,  Guy J. Laidig

IPC分类号： C07K5/107 ,  C07K5/117

CPC分类号： C07K5/1016 ,  A61K38/00 ,  A61K38/07 ,  C07K5/0812 ,  C07K5/0827 ,  C07K5/1008 ,  C07K5/1024

摘要： Peptide-based compounds including heteroatom-containing, three-membered rings efficiently and selectively inhibit specific activities of N-terminal nucleophile (Ntn) hydrolases. The activities of those Ntn having multiple activities can be differentially inhibited by the compounds described. For example, the chymotrypsin-like activity of the 20S proteasome may be selectively inhibited with the inventive compounds. The peptide-based compounds include an epoxide or aziridine, and functionalization at the N-terminus. Among other therapeutic utilities, the peptide-based compounds are expected to display anti-inflammatory properties and inhibition of cell proliferation.

公开(公告)号：US09878047B2

公开(公告)日：2018-01-30

申请号：US15065347

申请日：2016-03-09

申请人： Onyx Therapeutics, Inc.

发明人： Pasit Phiasivongsa ,  Gary W. Luehr ,  Ge Peng ,  Kolbot By ,  Shabbir T. Anik

IPC分类号： A61K38/00 ,  A61K47/00 ,  A61K47/48 ,  C07K5/083 ,  C07K5/107 ,  C07K5/097 ,  C07K5/117 ,  C07K7/06 ,  C07K5/065 ,  C07K5/103 ,  A61K38/07 ,  C07K5/113 ,  A61K47/60 ,  A61K47/54 ,  A61K38/06

CPC分类号： A61K47/64 ,  A61K38/06 ,  A61K38/07 ,  A61K47/549 ,  A61K47/60 ,  C07K5/06078 ,  C07K5/0806 ,  C07K5/081 ,  C07K5/0821 ,  C07K5/1008 ,  C07K5/1016 ,  C07K5/1021 ,  C07K5/1024 ,  C07K7/06

摘要： This disclosure features compounds that are useful as pro-drugs of epoxy ketone protease inhibitors.

公开(公告)号：US09795551B2

公开(公告)日：2017-10-24

申请号：US14315585

申请日：2014-06-26

申请人： L'OREAL

发明人： Jean-Marc Sabatier ,  Zhi Pan

IPC分类号： A61K38/00 ,  A61K8/64 ,  C07K5/117 ,  A61Q19/00 ,  A61Q5/00 ,  A23L3/3544 ,  C07K5/09 ,  A23L3/3526

CPC分类号： A61K8/64 ,  A23L3/3526 ,  A23L3/3544 ,  A23V2002/00 ,  A61K2800/10 ,  A61K2800/522 ,  A61Q5/00 ,  A61Q11/00 ,  A61Q19/00 ,  C07K5/0817 ,  C07K5/1024

摘要： A tetrapeptide having antioxidant activity is provided. The tetrapeptide has a structure comprising, in amino acid sequence from N-terminus to C-terminus: tryptophan-X-tyrosine-X; wherein X is arginine, lysine, histidine or any positively-charged amino acid derivative such as 5-hydroxylysine, ornithine, 2,4-diamino-butyrate and 2,3-diamino-propionate. Each amino acid of the sequence or its Homo-amino acid derivative is independently of the D configuration (D-stereoisomer) or of the L configuration (L-stereoisomer), and the C-terminal comprises one selected from the group consisting of carboxyl (—COOH), and carboxamide (—CONH2). A composition stabilized to oxidation or having antioxidant activity and a method for attenuating effects of free radicals on a keratinous material are also provided.

公开(公告)号：US20170275334A1

公开(公告)日：2017-09-28

申请号：US15618337

申请日：2017-06-09

申请人： RQX Pharmaceuticals, Inc.

发明人： Robert I. HIGUCHI ,  Tucker Curran ROBERTS ,  Peter Andrew SMITH ,  David CAMPBELL ,  Prasuna PARASELLI

IPC分类号： C07K7/06 ,  A61K38/07 ,  A61K45/06 ,  C07K5/11 ,  A61K38/06 ,  A61K38/08 ,  C07K5/08 ,  C07K5/113 ,  C07K5/103 ,  C07K5/117

CPC分类号： C07K7/06 ,  A61K38/06 ,  A61K38/07 ,  A61K38/08 ,  A61K45/06 ,  C07K5/08 ,  C07K5/1013 ,  C07K5/1019 ,  C07K5/1021 ,  C07K5/1024 ,  Y02A50/401 ,  Y02A50/47 ,  Y02A50/471 ,  Y02A50/473 ,  Y02A50/475 ,  Y02A50/478 ,  Y02A50/483

摘要： Provided herein are antibacterial compounds, wherein the compounds in some embodiments have broad spectrum bioactivity. The compounds provided herein can in other embodiments overcome the resistance conferred by single amino acid mutations at defined positions of bacterial Signal Peptidases (SPases) and in other embodiments provide for a broad spectrum of antibiotic bioactivity. Pharmaceutical compositions and methods for treatment using the compounds described herein are also provided.

公开(公告)号：US09751912B2

公开(公告)日：2017-09-05

申请号：US13729152

申请日：2012-12-28

申请人： TAO Health Life Pharma Co., Ltd.

发明人： Minako Hoshi

IPC分类号： A61K51/08 ,  A61K38/13 ,  A61K38/00 ,  C07K5/117 ,  A61K38/17 ,  A61K31/554 ,  G01N33/68 ,  C07K7/06 ,  C07K7/08 ,  C07K5/107 ,  C07K5/11

CPC分类号： C07K5/1024 ,  A61K31/554 ,  A61K38/00 ,  A61K38/13 ,  A61K38/1767 ,  A61K51/08 ,  C07K5/1016 ,  C07K5/1019 ,  C07K7/06 ,  C07K7/08 ,  G01N33/6896 ,  G01N2500/02 ,  G01N2800/2821

摘要： In one or a plurality of embodiments, there is provided a target molecule of amylospheroid, which is expressed in mature neurons and to which the amylospheroid binds to induce death of cells. Further, in one or a plurality of embodiments, there is provided a method and a substance for inhibiting death of mature neurons induced by the amylospheroid. In one aspect, the present disclosure relates to a use of Na+/K+-ATPase α3 as a binding target molecule of amylospheroid. In another aspect, the present disclosure relates to a method for suppressing death of mature neurons induced by the amylospheroid, including inhibiting protein-protein interaction between the amylospheroid and the Na+/K+-ATPase α3, and the like.

公开(公告)号：US20170157196A1

公开(公告)日：2017-06-08

申请号：US15239708

申请日：2016-08-17

申请人： HELIX BIOMEDIX, INC.

发明人： Scott M. Harris ,  Timothy J. Falla ,  Lijuan Zhang

IPC分类号： A61K38/07 ,  C07K5/117 ,  C07K5/103 ,  A61K9/00 ,  A61K9/06

CPC分类号： A61K38/07 ,  A61K8/64 ,  A61K9/0014 ,  A61K9/06 ,  A61K38/00 ,  A61K2121/00 ,  A61K2300/00 ,  A61Q19/00 ,  A61Q19/08 ,  C07K5/1002 ,  C07K5/1008 ,  C07K5/1024 ,  C07K14/78

摘要： Short biologically active tetrapeptides are disclosed that are comprised of the sequences GxxG and PxxP where G (glycine) and P (proline) are maintained and x is a variable amino acid. The peptides can be used singly or in combination to stimulate production of extracellular matrix proteins in skin. A rapid, low-cost method of producing heterogenous formulations of tetrapeptides is disclosed.