公开(公告)号：US10744203B2

公开(公告)日：2020-08-18

申请号：US16264364

申请日：2019-01-31

Applicant: Purdue Research Foundation ,  University of Utah Research Foundation

Inventor： Stewart Andrew Low ,  Philip S. Low ,  Christopher Galliford ,  Jindrich Kopecek ,  Jiyan Yang

IPC: A61K31/404 ,  C07D403/04 ,  C07D209/34 ,  C07D487/00 ,  A61K47/42 ,  A61L27/22 ,  A61L27/54 ,  C07K7/06 ,  C07K7/08 ,  A61P19/00 ,  A61K9/107 ,  A61M5/00

Abstract: Aspects of the present disclosure generally relate to compounds for targeting and healing bone fractures. Some of these compounds include a negatively charged oligopeptide comprising an acidic oligopeptide, a linker, which may be hydrolyzable or may be a substrate for the protease cathepsin K, and at least one molecule that promotes bone healing. In some compounds the molecule that promotes bone healing is an anabolic compound that inhibits GSK3β, in some compounds the molecule that promotes the healing of bone fracture is a pro-inflammatory agent such as PGE1. Other embodiments include methods of treating a bone fracture comprising administering a therapeutic amount of any one of the compounds disclosed herein.

公开(公告)号：US10736875B2

公开(公告)日：2020-08-11

申请号：US16126199

申请日：2018-09-10

Applicant: Ligand Pharmaceuticals, Inc.

Inventor： Lin Zhi ,  Keith Marschke ,  Virginia H. Grant ,  Steven L. Roach ,  Yixing Shen ,  Jason C. Pickens ,  Bijan Pedram ,  Cornelis Arjan van Oeveren ,  Lino J. Valdez ,  Andrew R. Hudson

IPC: C07D209/34 ,  A61K31/404 ,  C07D403/12 ,  C07D231/46 ,  C07D405/06 ,  A61K31/41 ,  A61K31/4152 ,  A61K31/4155 ,  A61K31/454 ,  A61K45/06 ,  A61N5/10 ,  C07D401/12 ,  C12Q1/18 ,  C12Q1/66 ,  C07D231/52

Abstract: Some embodiments include compositions and methods of using or identifying compounds that modulate the activity of the granulocyte colony-stimulating factor receptor (GCFR). Some embodiments include use of compounds to treat certain disorders, such as hematopoietic or neurological disorders.

公开(公告)号：US10703718B2

公开(公告)日：2020-07-07

申请号：US15893488

申请日：2018-02-09

Applicant: City of Hope

Inventor： Sangkil Nam ,  David Horne ,  Jun Xie

IPC: A61K31/404 ,  C07D209/40 ,  C07D403/04 ,  C07D209/34

Abstract: Disclosed herein are compositions and methods for treating cancer, FLT3-AML, and CML.

公开(公告)号：US10604484B2

公开(公告)日：2020-03-31

申请号：US15569313

申请日：2016-04-28

Applicant: Janssen Pharmaceutica NV

Inventor： Michael K. Ameriks ,  Suchitra Ravula ,  Bradley M. Savall ,  Devin M. Swanson ,  Jeannie M. Ziff ,  Brock T. Shireman

IPC: C07D209/34 ,  C07D401/04 ,  C07D403/12 ,  C07D405/12 ,  C07D417/12 ,  C07D401/10 ,  C07D403/10 ,  C07D413/10 ,  A61P37/00 ,  A61P25/28 ,  A61P31/18 ,  A61P23/00 ,  A61P25/18 ,  A61P25/24 ,  A61P25/00 ,  A61P25/16 ,  A61P25/06 ,  A61K31/4439

Abstract: Provided herein are compounds of Formula (I), and pharmaceutically acceptable salts, N-oxides, or solvates thereof, Also provided herein are pharmaceutical compositions, comprising compounds of Formula (I), and methods of using compounds of Formula (I).

公开(公告)号：US20190300480A1

公开(公告)日：2019-10-03

申请号：US16426406

申请日：2019-05-30

Applicant: THE UNIVERSITY OF BRITISH COLUMBIA ,  SIMON FRASER UNIVERSITY

Inventor： Paul RENNIE ,  Artem TCHERKASSOV ,  Robert N. YOUNG ,  Christophe M. ANDRE

IPC: C07D209/14 ,  C07D235/18 ,  C07D231/56 ,  C07D277/82 ,  C07D417/10 ,  C07D401/10 ,  C07D401/06 ,  C07D405/12 ,  C07D405/14 ,  C07D413/04 ,  C07D413/10 ,  C07D417/04 ,  C07C243/22 ,  C07D209/08 ,  C07D209/10 ,  C07D209/30 ,  C07D209/34 ,  C07D209/42 ,  C07D471/04 ,  C07D417/14 ,  C07D403/14 ,  C07D403/04 ,  C07D401/04 ,  C07D235/30

Abstract: This invention provides compound having a structure of Formulas: Uses of such compounds for treatment of various indications, including prostate cancer as well as methods of treatment involving such compounds are also provide.

公开(公告)号：US10370328B2

公开(公告)日：2019-08-06

申请号：US15565820

申请日：2016-04-28

Applicant: MUSC FOUNDATION FOR RESEARCH DEVELOPMENT ,  U.S. DEPARTMENT OF VETERANS AFFAIRS

Inventor： Craig C. Beeson ,  Christopher C. Lindsey ,  Baerbel Rohrer ,  Yuri Karl Peterson

IPC: C07D209/38 ,  C07D401/06 ,  C07D403/06 ,  C07D209/36 ,  C07D403/12 ,  C07D401/14 ,  C07D401/12 ,  C07D403/14 ,  C07D405/06 ,  C07D413/06 ,  C07D498/04 ,  A61P27/02 ,  C07D209/34 ,  C07D405/12 ,  C07F9/572

Abstract: Provided herein are compounds of the formula (I) as well as pharmaceutically acceptable salts thereof, wherein the substituents are as those disclosed in the specification. These compounds, and the pharmaceutical compositions containing them, are useful for the treatment of degenerative diseases and disorders.

公开(公告)号：US10308595B2

公开(公告)日：2019-06-04

申请号：US14768323

申请日：2014-02-14

Applicant: TECHNISCHE UNIVERSITAET BERLIN

Inventor： Roderich Suessmuth ,  Julian Kretz ,  Vivien Schubert ,  Alexander Pesic ,  Manuela Huegelland ,  Monique Royer ,  Stephane Cociancich ,  Philippe Rott ,  Dennis Kerwat ,  Stefan Graetz

IPC: C07C255/44 ,  C07C233/83 ,  C07C275/42 ,  C07D317/08 ,  C07D333/38 ,  C07C311/21 ,  C07D241/28 ,  C07D207/34 ,  C07D277/56 ,  C07D295/14 ,  C07D307/56 ,  C07F9/12 ,  C07C311/46 ,  C07C311/47 ,  C07C237/42 ,  C07C255/29 ,  C07C255/57 ,  C07C255/03 ,  C07F9/09 ,  C07D209/34 ,  C07D213/81 ,  C07D237/24 ,  C07D241/24 ,  C07D263/24 ,  C07D295/155 ,  C07D311/12 ,  C07D317/46 ,  C07F9/06

Abstract: Antibiotically active compounds characterized by general formula (I), wherein X1, BB, BC, BD, BE and X2 are building blocks with D1, D2, D3, D4 or D5 being linkers which include carbon, sulphur, nitrogen, phosphor and/or oxygen atoms and which are covalently connecting the moities BA and BB, BB and BC, BC and BD, BD and BE and BE and BF, respectively, and wherein in particular the building block BC comprises an amino acid derivative. The compounds for use in a method of treatment of diseases, in particular for use in a method of treatment of bacterial infections are also disclosed.

公开(公告)号：US20190144467A1

公开(公告)日：2019-05-16

申请号：US16249024

申请日：2019-01-16

Applicant: INTERMUNE, INC.

Inventor： Johnnie Y. Ramphal ,  Brad Owen Buckman ,  Kumaraswamy Emayan ,  John Beamond Nicholas ,  Scott D. Seiwert

IPC: C07D498/04 ,  C07D487/04 ,  C07C25/18 ,  C07D413/02 ,  C07D417/10 ,  C07D213/69 ,  C07D213/64 ,  C07D417/12 ,  C07D417/04 ,  C07D413/04 ,  C07D405/04 ,  C07D401/12 ,  C07D401/04 ,  C07D213/75 ,  C07D213/74 ,  C07D405/14 ,  C07D401/14 ,  C07D211/76 ,  C07D513/04 ,  C07D209/34 ,  C07D495/04 ,  C07D471/04 ,  C07C225/20 ,  C07D221/04 ,  C07D405/02

Abstract: Disclosed are pyridinone compounds, method for preparing these compounds, and methods for treating fibrotic disorders.

公开(公告)号：US10233177B2

公开(公告)日：2019-03-19

申请号：US15431265

申请日：2017-02-13

Applicant: Serentrix LLC

Inventor： Mauro Napoletano ,  Marcello Trevisani ,  Maria Giovanna Pavani ,  Francesca Fruttarolo

IPC: C07D413/14 ,  C07D263/58 ,  C07D209/34 ,  C07D235/26 ,  C07D265/36 ,  C07D401/12 ,  C07D403/12 ,  C07D405/12 ,  C07D401/14 ,  C07D413/12

Abstract: The invention discloses compounds of formula I wherein Y is a group of formula A, B, C, D, or E: and W, Q, n, R1, R2, R3, U1-U5, J and K have the meanings given in the description. The compounds of formula I are TRPV1 antagonists and are useful as active ingredients of pharmaceutical compositions for the treatment of pain and other conditions ameliorated by the inhibition of the vanilloid receptor TRPV1.

公开(公告)号：US20180339965A1

公开(公告)日：2018-11-29

申请号：US15988781

申请日：2018-05-24

Applicant: RESEARCH & BUSINESS FOUNDATION SUNGKYUNKWAN UNIVERSITY

Inventor： In Su KIM ,  Hyung Sik KIM

IPC: C07D209/34 ,  A61P35/00

CPC classification number: C07D209/34 ,  A61P35/00

Abstract: The present invention relates to a novel oxindole derivative having anticancer activity, a preparation method thereof, and a method for treating cancer using the same. More specifically, the present invention relates to an oxindole derivative produced as a result of CH alkylation and subsequent intramolecular cyclization reaction using a rhodium (III) catalyst, a preparation method of the same, and a method for treating cancer containing the same as an active ingredient. The novel oxindole derivatives according to the present invention have excellent anticancer activity against various human cancer cell lines and are expected to be useful for the treatment of cancer. In addition, the preparation method of an oxindole derivative using the rhodium (III) catalyst of the present invention can be applied and introduced into a wide range of functional groups, and is a reaction having positional selectivity and chemical selectivity. As a reaction for synthesizing a new drug or a compound having biological activity, it will be useful.