Abstract: A compound of the general formula X-[Q-W—(CH?CH)n—(CH2)2-L]m (I) in which X represents a polymer; Q represents a linking group; W represents an electron-withdrawing group; n represents 0 or an integer of from 1 to 4; L represents a leaving group; and m represent an integer of from 1 to 8. The compounds find use in the conjugation of biological molecules.
Abstract: The present invention relates to dipeptide enkephalin analogues of Formula (I) and their tautomers, ionic forms and pharmaceutically acceptable salts, and their use in medicine, in particular as opioid agonists.
Abstract: The present invention is directed to polymeric materials comprising biodegradable, dioxanone-based copolymers and implantable devices (e.g., drug-delivery stents) formed of such materials. The polymeric materials can also contain at least one additional biocompatible moiety, at least one non-fouling moiety, at least one biobeneficial material, at least one bioactive agent, or a combination thereof. The polymeric materials are designed to improve the mechanical, physical and biological properties of implantable devices formed thereof.
Abstract: The invention provides methods for the identification of small molecules that inhibit MUC1 oligomerization, and the functions flowing therefrom. In addition, small molecules that prevent MUC1 oligomerization are disclosed. Identified molecules will find use in treating a variety of MUC1-related inflammatory conditions, including MUC1-related cancers.
Type:
Grant
Filed:
March 10, 2011
Date of Patent:
February 10, 2015
Assignees:
Dana-Farber Cancer Institute, Inc., Genus Oncology, LLC
Abstract: The invention provides a method for inhibiting melanin formation composition by applying a glycine derivative, having a structure shown in the following general equation (I): wherein R1 represents a C1˜C4 alkyl group; R2 represents a hydrogen atom or a methyl group; and n represents an integer of 1˜6.
Abstract: ClotGel is a single-component hemostatic agent designed for use as an adjunct or primary treatment in moderate intraoperative hemorrhage and in trauma. It can be applied topically to the wound either on the skin in a laparatomy or as non-invasive manner in surgical procedures. Its crosslinking technology generates an adhesive stable fibrin clot using a single component (fibrin II) required for hemostasis. The agent is a mixture of lyophilized polymerized fibrin II and fibrin II monomer which is polymerized and stabilized when in contact with the blood. The attachment properties of the gel, as well as the rapid formation of a fibrin clot, ensures that a strong stable fibrin clot is formed within 1 minute of application.
Abstract: In general, the invention relates to methods of synthesizing AbA derivatives that are useful for treating infection and amenable to further chemical elaboration. These novel methods are scalable for industrial production and employ safer, simpler, and more efficient process conditions. Furthermore, the invention also provides novel compounds and intermediates useful for implementing the methods described herein and/or for the treatment of infection.
Abstract: The invention relates to the compounds of formula (I) and physiologically acceptable salts thereof. The compounds are suitable, e.g., for treating hyperglycemia.
Type:
Grant
Filed:
March 7, 2012
Date of Patent:
December 2, 2014
Assignee:
Sanofi
Inventors:
Thomas Boehme, Christian Engel, Stefan Guessregen, Torsten Haack, Gerhard Kretzschmar, Kurt Ritter, Georg Tschank
Abstract: The invention relates to the compounds of formula (I) and to the physiologically acceptable salts thereof. Said compounds are suitable e.g. for the treatment of hyperglycemia.
Type:
Grant
Filed:
March 7, 2012
Date of Patent:
November 25, 2014
Assignee:
Sanofi
Inventors:
Thomas Boehme, Christian Engel, Stefan Guessregen, Torsten Haack, Kurt Ritter, Georg Tschank
Abstract: The present invention relates to substituted quinazolines of formula (I): wherein X and Y are defined as in claim 1, the tautomers, stereoisomers, mixtures and salts thereof, which have valuable pharmacological properties, particularly an inhibitory effect on the activity of the enzyme dipeptidylpeptidase-IV (DPP-IV).
Type:
Grant
Filed:
July 13, 2012
Date of Patent:
November 11, 2014
Assignee:
Boehringer Ingelheim International GmbH
Inventors:
Waldemar Pfrengle, Markus Frank, Thomas Klein
Abstract: The present invention provides a compound of formula I; or a pharmaceutically acceptable salt thereof, wherein R1, R2, R3, R4, R5, B, X, m and n are defined herein. The invention also relates to a method for manufacturing the compounds of the invention, and its therapeutic uses. The present invention further provides pharmaceutical composition of compounds of the invention, and a combination of pharmacologically active agents and a compound of the invention.
Type:
Grant
Filed:
November 10, 2011
Date of Patent:
November 4, 2014
Assignee:
Novartis AG
Inventors:
Rajeshri Ganesh Karki, Toshio Kawanami, Gary Michael Ksander, Qian Liu, Muneto Mogi, Nikolaus Schiering, Robert Sun
Abstract: The invention relates to the compounds of formula (I) and to the physiologically acceptable salts thereof. Said compounds are suitable e.g. for the treatment of hyperglycemia.
Type:
Grant
Filed:
March 7, 2012
Date of Patent:
October 28, 2014
Assignee:
Sanofi
Inventors:
Thomas Boehme, Christian Engel, Stefan Guessregen, Torsten Haack, Kurt Ritter, Georg Tschank
Abstract: Compounds of the formula I wherein R2a and R2b are independently H, halo, C1-C4alkyl, C1-C4haloalkyl or C1-C4alkoxy, or R2a and R2b together with the carbon atom to which they are attached form a C3-C6cycloalkyl; R3 is a C5-C10 alkyl, optionally substituted with 1-3 substituents independently selected from halo, C1-C4haloalkyl, C1-C4alkoxy, C1-C4haloalkoxy; or R3 is a C2-C4alkyl chain with at least 2 chloro or 3 fluoro substituents; or R3 is C3-C7cycloalkylmethyl, optionally substituted with 1-3 substituents independently selected from C1-C4alkyl, halo, C1-C4haloalkyl, C1-C4alkoxy, C1-C4haloalkoxy; R4 is C1-C6alkyl, C1-C6haloalkyl, C1-C6alkoxy, C1-C6haloalkoxy, C1-C6alkylamino, C1-C6dialkylamino or; R4 is Het or Carbocyclyl, either of which is optionally substituted with 1-3 substituents R4 is Het, carbocyclyl, C1-C6alkyl, C1-C6haloalkyl, C1-C6alkoxy or C1-C6haloalkoxy; n is 1, 2 or 3; for the use in the prophylaxis or treatment of a disorder characterised by inappropriate expression or activation of ca
Type:
Grant
Filed:
June 16, 2011
Date of Patent:
October 14, 2014
Assignee:
Medivir UK Ltd
Inventors:
Susana Ayesa, Urszula Grabowska, Ellen Hewitt, Daniel Jonsson, Bjorn Klasson, Pia Kahnberg, Stina Lundgren, Jan Tejbrant, Daniel Wiktelius
Abstract: Biocompatible macromonomers, hydrogels, methods of synthesis and methods of use thereof are provided. The biocompatible hydrogels of the present invention are prepared using native chemical ligation (NCL), in which a thioester readily reacts with a N-terminal thiol (cysteine) through transesterification and rearrangement to form an amide bond through a five-member ring intermediate.
Type:
Grant
Filed:
April 21, 2008
Date of Patent:
September 23, 2014
Assignee:
Northwestern University
Inventors:
Phillip B Messersmith, Bi-Huang Hu, Jing Su
Abstract: The present invention relates to polyamides capable of inhibiting ARE-, GRE- and ERE-mediated gene regulation in cells. The invention also relates to methods to treat diseases related to ARE-, GRE- and ERE-mediated gene regulation.
Abstract: The invention relates to compounds of formula (I) and to the physiologically compatible salts thereof. Said compounds are suitable, for example, for treating hyperglycemia.
Type:
Grant
Filed:
March 7, 2012
Date of Patent:
September 9, 2014
Assignee:
SANOFI
Inventors:
Thomas Boehme, Christian Engel, Stefan Guessregen, Torsten Haack, Kurt Ritter, Georg Tschank
Abstract: The invention relates to compounds of formula (I) and to the physiologically compatible salts thereof. Said compounds are suitable, for example, for treating hyperglycemia.
Type:
Grant
Filed:
March 7, 2012
Date of Patent:
September 9, 2014
Assignee:
Sanofi
Inventors:
Thomas Boehme, Christian Engel, Stefan Guessregen, Torsten Haack, Kurt Ritter, Georg Tschank
Abstract: This invention comprises peptides, methods and a kit for identifying DNA fragmentation in non-viable sperm. Specific peptide sequences are claimed that bind to ssDNA and fragmented DNA.
Type:
Grant
Filed:
November 18, 2011
Date of Patent:
August 26, 2014
Inventors:
Dagan Wells, Jacques Cohen, George Pieczenik
Abstract: The invention relates to the compounds of formula (I) and to the physiologically acceptable salts thereof. Said compounds are suitable e.g. for the treatment of hyperglycemia.
Type:
Grant
Filed:
March 7, 2012
Date of Patent:
August 19, 2014
Assignee:
Sanofi
Inventors:
Thomas Boehme, Kurt Ritter, Christian Engel, Torsten Haack, Stefan Guessregen, Georg Tschank
Abstract: A nanostructure composed of a plurality of peptides, each peptide containing at least one aromatic amino acid, whereby one or more of these peptides is end-capping modified, is disclosed. The nanostructure can take a tubular, fibrillar, planar or spherical shape, and can encapsulate, entrap or be coated by other materials. Methods of preparing the nanostructure, and devices and methods utilizing same are also disclosed.