公开(公告)号：US09851363B2

公开(公告)日：2017-12-26

申请号：US14784484

申请日：2014-04-18

Applicant: CENTRE NATIONAL DE LA RECHERCHE SCIENTIFIQUE (CNRS) ,  UNIVERSITE PARIS DESCARTES ,  INSTITUT NATIONAL DE LA SANTE ET DE LA RECHERCHE MEDICALE (INSERM)

Inventor： Veronique Baud ,  Katy Billot

IPC: G01N33/68 ,  G01N33/574 ,  C07K16/18

CPC classification number: G01N33/6872 ,  C07K16/18 ,  G01N33/57484 ,  G01N2333/4703 ,  G01N2440/14 ,  G01N2500/04 ,  G01N2500/10

Abstract: The present Inventors demonstrated that the RelB subunit of NFκB plays a crucial role in promoting cell migration. More precisely, they identified that this pro-migratory activity is mediated by the activation of the NFκB pathway through RelB phosphorylation at serine 472. In a first aspect, the present invention proposes to monitor the activation of the NFκB pathway by following the phosphorylation status of said serine. Also, the present invention discloses methods and kits for prognosing the evolution of a disease involving cell migration in a subject—treated or not—suffering thereof, based on the detection of said RelB-S472 phosphorylation.

公开(公告)号：US09844546B2

公开(公告)日：2017-12-19

申请号：US14713085

申请日：2015-05-15

Applicant: OXFORD UNIVERSITY INNOVATION LIMITED

Inventor： Patrick Henry Maxwell ,  Christopher William Pugh ,  Peter John Ratcliffe ,  Christopher Joseph Schofield

IPC: C07K16/18 ,  C07K16/40 ,  C07K14/47 ,  A61K31/455 ,  G01N33/573 ,  C12N9/02 ,  C12Q1/26 ,  C07C235/80 ,  C07C323/60 ,  C07C327/32 ,  C07D213/80 ,  C07D213/81 ,  C07D213/82 ,  A61K31/137 ,  A61K31/166 ,  A61K31/185 ,  A61K31/198 ,  A61K31/21 ,  A61K31/225 ,  A61K31/44 ,  A61K31/192 ,  A61K31/195 ,  A61K31/197 ,  A61K31/24 ,  A61K31/327 ,  A61K31/4412 ,  A61K31/14 ,  A61K31/194 ,  A61K31/221 ,  C07K14/435 ,  C12N9/00 ,  A61K39/395 ,  A61K38/00

CPC classification number: A61K31/455 ,  A01K2217/05 ,  A61K31/137 ,  A61K31/14 ,  A61K31/165 ,  A61K31/166 ,  A61K31/185 ,  A61K31/192 ,  A61K31/194 ,  A61K31/195 ,  A61K31/197 ,  A61K31/198 ,  A61K31/21 ,  A61K31/221 ,  A61K31/223 ,  A61K31/225 ,  A61K31/235 ,  A61K31/24 ,  A61K31/265 ,  A61K31/327 ,  A61K31/44 ,  A61K31/4412 ,  A61K38/00 ,  A61K39/3955 ,  C07C235/80 ,  C07C323/60 ,  C07C327/32 ,  C07D213/80 ,  C07D213/81 ,  C07D213/82 ,  C07K14/4702 ,  C07K16/40 ,  C07K2317/30 ,  C12N9/0071 ,  C12Q1/26 ,  C12Q1/34 ,  G01N33/573 ,  G01N2333/90245 ,  G01N2500/04 ,  G01N2500/20

Abstract: A novel class of hydroxylases is described having the amino acid sequence of SEQ ID NO: 2, 4, 6 and 8, and variants and fragments thereof having HIF hydroxylation activity. The polypeptides of the invention have in particular prolyl hydroxylase activity. An assay method monitors the interaction of the HIF hydroxylase with a substrate. Modulators of HIF hydroxylase are provided for use in the treatment of a condition associated with increased or decreased HIF levels or activity or for the treatment of a condition where it is desirable to modulate HIF levels or activity.

公开(公告)号：US20170356024A1

公开(公告)日：2017-12-14

申请号：US15524181

申请日：2015-11-04

Applicant: BRANDEIS UNIVERSITY

Inventor： DOROTHEE KERN

IPC: C12Q1/48 ,  G06F19/00

CPC classification number: C12Q1/485 ,  G01N33/557 ,  G01N33/573 ,  G01N2333/91205 ,  G01N2500/00 ,  G01N2500/04 ,  G01N2500/20 ,  G16C10/00

Abstract: In one aspect, the present invention provides a method of selecting or identifying an agent that inhibits a target protein having an active site. In another aspect, the invention provides a method of selecting an agent that inhibits a target protein having an active site for further optimization. In some embodiments, the methods comprise measuring or predicting stability of an induced fit conformation of an agent contacted to an active site of the protein, wherein the agent is selected if the stability of the induced fit conformation of the agent contacted to the active site of the protein is increased relative to a reference stability.

公开(公告)号：US20170355749A1

公开(公告)日：2017-12-14

申请号：US15528387

申请日：2015-11-20

Applicant: CYTONICS CORPORATION

Inventor： Lewis HANNA ,  John David LAUGHLIN ,  Shawn Robert BROWNING

IPC: C07K14/81 ,  A61K38/57 ,  A61K9/00 ,  C12Q1/37 ,  A61K45/06 ,  C12P19/34

CPC classification number: C07K14/811 ,  A61K9/0019 ,  A61K38/57 ,  A61K45/06 ,  C12P19/34 ,  C12Q1/37 ,  G01N2333/811 ,  G01N2500/04 ,  G01N2500/20

Abstract: A2M polypeptide compositions containing a non-natural bait region are disclosed. Methods of producing wild-type and variant A2M polypeptides and polynucleotides containing a non-natural bait region are also disclosed. The bait regions of the variant A2M polypeptides demonstrate enhanced protease inhibitory characteristics compared to wild-type A2M. Variant A2M polypeptides that demonstrate longer half-lives upon administration to an organism compared to wild-type A2M are disclosed. The A2M compositions are useful in treating a number of diseases and conditions including inflammation, chronic wounds, and diseases with a pathology associated with proteases.

公开(公告)号：US09840533B2

公开(公告)日：2017-12-12

申请号：US14787611

申请日：2014-04-29

Applicant: Memorial Sloan Kettering Cancer Center ,  The Rockefeller University ,  Rutgers, The State University of New Jersey ,  University of Bonn

Inventor： Dinshaw Patel ,  Thomas Tuschl ,  Manuel Ascano, Jr. ,  Yang Wu ,  Yizhou Liu ,  Winfried Barchet ,  Gunther Hartmann ,  Thomas Zillinger ,  Roger Jones ,  Barbara L. Gaffney ,  Pu Gao

IPC: C07H21/00 ,  A61K31/522 ,  C07F9/6574 ,  C12Q1/48 ,  G06F19/16 ,  G06F19/18 ,  G06K9/00 ,  G06K9/46 ,  A61K47/55

CPC classification number: C07H21/00 ,  A61K31/522 ,  A61K47/55 ,  C07F9/65746 ,  C12Q1/485 ,  C12Y207/07 ,  G01N2500/04 ,  G01N2500/10 ,  G06F19/16 ,  G06F19/18 ,  G06K9/00147 ,  G06K9/46

Abstract: The present disclosure provides, among other things, novel cyclic-GMP-AMP (cGAMP) analogs, mimics, mimetics and variants, and compositions and kits thereof; methods of using the compounds as described herein for treating cancer, and immune disease, disorders, or conditions; methods of using the compounds as described herein for modulating cGAS and STING; and methods of designing or characterizing a cGAS modulator.

公开(公告)号：US20170349589A9

公开(公告)日：2017-12-07

申请号：US14972482

申请日：2015-12-17

Applicant: AbbVie Inc.

Inventor： Yujia Dai ,  William McClellan ,  Mike Michaelides ,  Ramzi Sweis ,  Noel Wilson ,  Justin Dietrich

IPC: C07D473/34 ,  C07D519/00 ,  C12Q1/48

CPC classification number: C07D473/34 ,  C07D519/00 ,  C12Q1/48 ,  G01N2333/91017 ,  G01N2500/04

Abstract: The invention provides for compounds of formula (I) wherein R1, R2, R3, R4, R5, and R6 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 mediated and modulated by SUV420H1. Also provided are pharmaceutical compositions comprised of one or more compounds of formula (I).

公开(公告)号：US20170335394A1

公开(公告)日：2017-11-23

申请号：US15477206

申请日：2017-04-03

Applicant: The Brigham and Women's Hospital, Inc. ,  Celera Corporation

Inventor： PAUL M. RIDKER ,  Daniel Chasman ,  Dov Shiffman

IPC: C12Q1/68 ,  G01N33/92 ,  A61K31/616

CPC classification number: C12Q1/6883 ,  A61K31/616 ,  C12Q1/6876 ,  C12Q2600/106 ,  C12Q2600/136 ,  C12Q2600/156 ,  C12Q2600/158 ,  C12Q2600/172 ,  G01N33/92 ,  G01N2333/775 ,  G01N2500/04 ,  G01N2800/32 ,  G01N2800/50 ,  G01N2800/52

Abstract: This invention relates to nucleotide polymorphisms in the human Apo(a) gene and to the use of Apo(a) nucleotide polymorphisms in identifying whether a human subject will respond or not to treatment with acetylsalicylic acid.

公开(公告)号：US20170305899A1

公开(公告)日：2017-10-26

申请号：US15342056

申请日：2016-11-02

Applicant: Fred Hutchinson Cancer Research Center ,  The Scripps Research Institute

Inventor： Gerald R. Smith ,  Susan K. Amundsen ,  Ahmet C. Karabulut ,  Thomas D. Bannister ,  Reji Narayanan Nair

IPC: C07D471/04 ,  A61K31/497 ,  A61K31/5365 ,  C12Q1/44 ,  A61K31/495 ,  C12Q1/18 ,  A61K31/519

CPC classification number: C07D471/04 ,  A61K31/495 ,  A61K31/497 ,  A61K31/519 ,  A61K31/5365 ,  C12Q1/18 ,  C12Q1/44 ,  G01N2333/922 ,  G01N2500/04 ,  G01N2500/10 ,  Y02A50/401 ,  Y02A50/469 ,  Y02A50/47 ,  Y02A50/471 ,  Y02A50/473 ,  Y02A50/475 ,  Y02A50/478 ,  Y02A50/481

Abstract: Disclosed herein are compounds and methods for inhibiting bacterial DNA repair enzymes, including AddAB and RecBCD helicase-nucleases. Pharmaceutical compositions and methods for treating a subject with an antibacterial agent are also disclosed herein.

公开(公告)号：US09778249B2

公开(公告)日：2017-10-03

申请号：US15514683

申请日：2015-09-25

Applicant: UNIVERSITY OF HOUSTON SYSTEM

Inventor： Shoujun Xu ,  Qiongzheng Hu ,  Yuhong Wang ,  Te-Wei Tsai

IPC: G01N33/553 ,  C12Q1/68 ,  G01N33/53

CPC classification number: G01N33/5308 ,  C12Q1/6804 ,  G01N33/54333 ,  G01N2500/04 ,  G01N2500/20

Abstract: Methods of quantifying the efficiency of a drug molecule for its targeted receptor, using a differential binding force to quantify the efficiency of a drug molecule to its targeted receptor.

公开(公告)号：US20170267651A1

公开(公告)日：2017-09-21

申请号：US15505898

申请日：2014-08-22

Applicant: Duke University ,  The Regents of the University of California

Inventor： Wolfgang LIEDTKE ,  Martin STEINHOFF ,  Farshid GUILAK

IPC: C07D277/20 ,  A01K67/027 ,  G01N33/68 ,  A61K9/00 ,  C07K14/705 ,  C07D519/00 ,  A61K49/00

CPC classification number: C07D277/20 ,  A01K67/0276 ,  A01K2217/075 ,  A01K2217/206 ,  A01K2227/105 ,  A01K2267/0356 ,  A61K9/0014 ,  A61K31/426 ,  A61K31/4439 ,  A61K49/0008 ,  C07D519/00 ,  C07K14/705 ,  G01N33/6872 ,  G01N33/6881 ,  G01N2333/4703 ,  G01N2500/04 ,  G01N2500/10

Abstract: Provided are methods of treating and/or preventing dermatological disorders. Provided are methods of reducing skin inflammation, reducing pain, and/or reducing itch in a subject in need thereof. The methods may include administering to the subject an effective amount of a TRPA1 and/or TRPV4 inhibitor. Further provided are compositions including a TRPA1 and/or TRPV4 inhibitor compound in combination with a carrier, vehicle, or diluent that is suitable for topical application.