Additional Hetero Ring Attached Directly Or Indirectly To The Piperazine Ring By Nonionic Bonding Patents (Class 514/252.13)
  • Patent number: 10300056
    Abstract: The disclosures herein relate to novel compounds of formula wherein R1, R2, R3 and R4 are as defined herein, and their use in treating, preventing, ameliorating, controlling or reducing cerebrovascular or vascular disorders associated with CGRP receptor function.
    Type: Grant
    Filed: September 25, 2017
    Date of Patent: May 28, 2019
    Assignee: Heptares Therapeutics Limited
    Inventors: John Andrew Christopher, Miles Stuart Congreve, Sarah Joanne Bucknell, Francesca Deflorian, Mark Pickworth, Jonathan Stephen Mason
  • Patent number: 10213392
    Abstract: The invention relates to the manufacturing and use of pharmaceutical compositions of medicines (ophthalmic preparations) comprising a mitochondria-addressed antioxidant and a set of auxiliary substances providing effective treatment for ophthalmological diseases in humans and animals.
    Type: Grant
    Filed: July 12, 2017
    Date of Patent: February 26, 2019
    Assignee: MITOTECH SA
    Inventor: Maxim V. Skulachev
  • Patent number: 10195207
    Abstract: The invention relates to a serotonin receptor (5-HTR) inhibitor selected from the group consisting of a type 1 5-HTR inhibitor and a type 2 5-HTR inhibitor for use in the prevention and/or treatment of a haematological malignancy. Additionally, the invention relates to in vitro methods for the identification or isolation of a malignant cell from a haematological malignancy or for diagnosing a haematological malignancy based on detecting the expression of type 1 5-HTR and/or type 2 5-HTR. Furthermore, the invention relates to in vitro methods for determining the prognosis, for monitoring the effect of a therapy or for designing a customized therapy in a subject suffering from a haematological malignancy based on determining the levels of type 1 5-HTR and/or type 2 5-HTR.
    Type: Grant
    Filed: June 26, 2015
    Date of Patent: February 5, 2019
    Assignee: INSTITUT DE RECERCA CONTRA LA LEUCÈMIA JOSEP CARRERAS
    Inventor: Ruth Muñoz Risueño
  • Patent number: 10150735
    Abstract: The present invention provides low hygroscopic forms of aripiprazole and processes for the preparation thereof which will not convert to a hydrate or lose their original solubility even when a medicinal preparation containing the anhydrous aripiprazole crystals is stored for an extended period.
    Type: Grant
    Filed: February 18, 2015
    Date of Patent: December 11, 2018
    Assignee: Otsuka Pharmaceutical Co., Ltd.
    Inventors: Takuji Bando, Satoshi Aoki, Junichi Kawasaki, Makoto Ishigami, Youichi Taniguchi, Tsuyoshi Yabuuchi, Kiyoshi Fujimoto, Yoshihiro Nishioka, Noriyuki Kobayashi, Tsutomu Fujimura, Masanori Takahashi, Kaoru Abe, Tomonori Nakagawa, Koichi Shinhama, Naoto Utsumi, Michiaki Tominaga, Yoshihiro Ooi, Shohei Yamada, Kenji Tomikawa
  • Patent number: 10137081
    Abstract: A drug delivery device comprising a non-erodible, non-porous housing member defining a reservoir is provided. The reservoir is loaded with a dry formulation of a selected salt of a neuroleptic agent. The housing member has one or more porous partitions, where the pores of the partitions are sufficiently small to retain the insoluble powder particles within the reservoir yet large enough to allow diffusion of the active agent once the device is hydrated. A therapeutic dose of the drug is released from the device at a constant rate over a period of approximately 2-6 months.
    Type: Grant
    Filed: September 27, 2013
    Date of Patent: November 27, 2018
    Assignee: Delpor, Inc.
    Inventor: Gregory Alan Watkins
  • Patent number: 9988354
    Abstract: Provided are omecamtiv mecarbil dihydrochloride salt forms, compositions and pharmaceutical formulations thereof, and methods for their preparation and use.
    Type: Grant
    Filed: March 14, 2014
    Date of Patent: June 5, 2018
    Assignee: AMGEN INC.
    Inventors: Sheng Cui, Henry Morrison, Karthik Nagapudi, Shawn Walker, Charles Bernard, Karl Bennett Hansen, Neil Fred Langille, Alan Martin Allgeier, Steven Mennen, Jacqueline Woo
  • Patent number: 9951015
    Abstract: Provided are certain pharmaceutical formulations of omecamtiv mecarbil and methods for their preparation and use.
    Type: Grant
    Filed: March 14, 2014
    Date of Patent: April 24, 2018
    Assignee: AMGEN INC.
    Inventors: Mingda Bi, Robert Kuehl
  • Patent number: 9926286
    Abstract: The present invention provides a new intermediate II and a method for synthesizing the same. The method comprises: (a) firstly diazotizing a compound of formula I as a raw material, and then halogenating to obtain an intermediate II; and (b) reacting the intermediate II with a compound III to obtain a compound IV, hydrolyzing the obtained compound IV directly without being separated to obtain Vortioxetine represented by compound V. The intermediate II can be used for synthesizing Vortioxetine.
    Type: Grant
    Filed: March 25, 2015
    Date of Patent: March 27, 2018
    Assignees: SHANGHAI SYNCORES TECHNOLOGIES INC. LTD., ZHEJIANG HUAHAI PHARMACEUTICAL CO., LTD
    Inventors: Caide Tang, Gang Wang, Boyu Wang, Luning Huang, Eric Gu
  • Patent number: 9801877
    Abstract: The present invention provides a compound of Formula I or Formula II: enantiomer, diastereomer, prodrug, solvate, metabolite, or pharmaceutically acceptable salt thereof, wherein constituent variables are provided herein. The compounds of Formula I and II are modulators of metalloproteases and are useful in treating diseases associated with metalloprotease activity such as arthritis, cancer, cardiovascular disorders, skin disorders, inflammation and allergic conditions.
    Type: Grant
    Filed: July 7, 2016
    Date of Patent: October 31, 2017
    Assignees: Incyte Corporation, Incyte Holdings Corporation
    Inventors: Wenqing Yao, Jincong Zhuo, Meizhong Xu, Fenglei Zhang, Brian W. Metcalf
  • Patent number: 9795604
    Abstract: Described herein are methods for treating and preventing graft versus host disease using ACK inhibitors. The methods include administering to an individual in need thereof an ACK inhibitor such as ibrutinib for treating and preventing graft versus host disease.
    Type: Grant
    Filed: October 24, 2014
    Date of Patent: October 24, 2017
    Assignee: Pharmacyclics LLC
    Inventors: John C. Byrd, Jason A. Dubovsky, Natarajan Muthusamy, Amy Jo Johnson, David Miklos
  • Patent number: 9795575
    Abstract: The present invention provides methods for treating and/or preventing mucositis with one or more compounds, or pharmaceutically acceptable salts thereof, disclosed herein, or compositions comprising the same.
    Type: Grant
    Filed: August 17, 2016
    Date of Patent: October 24, 2017
    Assignee: Innovation Pharmaceuticals Inc.
    Inventors: Richard W. Scott, Bozena Korczak
  • Patent number: 9695122
    Abstract: The present invention relates to compounds and processes for preparing compounds of Formula (I), including compounds such as trans-7-oxo-6-(sulphooxy)-1,6-diazabicyclo[3,2,1]octane-2-carboxamide and salts thereof (e.g., NXL-104).
    Type: Grant
    Filed: February 10, 2016
    Date of Patent: July 4, 2017
    Assignee: Forest Laboratories Holdings Ltd.
    Inventors: Melanie Simone Ronsheim, Saibaba Racha, Graham Richard Lawton, Shao Hong Zhou, Yuriy B. Kalyan, Michael Golden, David Milne, Alexander Telford, Janette Cherryman, Alistair Boyd, Andrew Phillips, Mahendra G. Dedhiya
  • Patent number: 9562044
    Abstract: Thiazole derivatives having pyrazine-2-carbonylamino substituted at the 2-position of the following formula (I): are excellent muscarinic M3 receptor positive allosteric modulators, and are useful for treating bladder or urinary tract diseases, related to bladder contraction by a muscarinic M3 receptor. The 2-acylaminothiazole derivatives and salts thereof can be used for treating bladder or urinary tract diseases, related to bladder contraction by a muscarinic M3 receptor, for example, voiding dysfunctions such as underactive bladder.
    Type: Grant
    Filed: February 27, 2014
    Date of Patent: February 7, 2017
    Assignee: Astellas Pharma Inc.
    Inventors: Taisuke Takahashi, Jun Maeda, Yusuke Inagaki, Kenji Negoro, Hiroaki Tanaka, Kazuhiro Yokoyama, Hajime Takamatsu, Takanori Koike, Issei Tsukamoto
  • Patent number: 9512073
    Abstract: Described herein are compounds and compositions characterized, in certain embodiments, by conjugation of various groups, such as lipophilic groups, to an amino or amide group of an amino acid, a linear or cyclic peptide, a linear or cyclic polypeptide, or structural isomer thereof, to provide compounds of the present invention, collectively referred to herein as “APPLs”. Such APPLs are deemed useful for a variety of applications, such as, for example, improved nucleotide delivery. Exemplary APPLs include, but are not limited to, compounds of Formula (I), (II), (III), (IV), (V), and (VI), and salts thereof, as described herein: wherein m, n, p, R?, R1, R2, R3, R4, R5, R8, Z, W, Y, and Z are as defined herein.
    Type: Grant
    Filed: October 26, 2012
    Date of Patent: December 6, 2016
    Assignee: Massachusetts Institute of Technology
    Inventors: Yizhou Dong, Kevin Thomas Love, Robert S. Langer, Daniel Griffith Anderson, Delai Chen, Yi Chen, Arturo Jose Vegas, Akinleye C. Alabi, Yunlong Zhang
  • Patent number: 9469646
    Abstract: Agents for modulating methyl modifying enzymes, compositions and uses thereof are provided herein.
    Type: Grant
    Filed: August 28, 2015
    Date of Patent: October 18, 2016
    Assignee: Constellation Pharmaceuticals, Inc.
    Inventors: Brian K. Albrecht, James Edmund Audia, Les A. Dakin, Victor S. Gehling, Jean-Christophe Harmange, Christopher G. Nasveschuk, Rishi G. Vaswani
  • Patent number: 9458134
    Abstract: The invention provides novel heterocyclic amines according to Formula (I) their manufacture and use for the treatment of hyperproliferative diseases, such as cancer.
    Type: Grant
    Filed: March 10, 2014
    Date of Patent: October 4, 2016
    Assignee: Merck Patent GmbH
    Inventors: Ruoxi Lan, Xiaoling Chen, Yufang Xiao, Bayard R. Huck, Andreas Goutopoulos
  • Patent number: 9440958
    Abstract: The present invention provides compounds of the formula I: its enantiomers, diastereomers, racemic mixtures thereof, prodrugs, crystalline forms, non-crystalline forms, amorphous forms thereof, solvates thereof, metabolites thereof, and pharmaceutically acceptable salts, wherein the ring A substituent groups are fully defined in the following disclosure. The compounds of formula I are inhibitors of metalloproteases such as matrix metalloproteases and sheddases, and are useful in treating diseases such as rheumatoid arthritis, psoriasis, neoplastic diseases, allergies and all those diseases wherein inhibition of MMPs is desirable.
    Type: Grant
    Filed: October 3, 2014
    Date of Patent: September 13, 2016
    Assignees: Incyte Corporation, Incyte Holdings Corporation
    Inventors: Yun-Long Li, Jincong Zhuo, David M. Burns, Wenqing Yao, Ravi Kumar Jalluri
  • Patent number: 9428456
    Abstract: The present invention relates to 1-[m-carboxamido(hetero)aryl-methyl]-heterocycyl-carboxamide compounds of formula (I) wherein X, Ar1, R1, R2, R3, R4, R5a, R5b and p are as described in the description, to their preparation, to pharmaceutically acceptable salts thereof, and to their use as pharmaceuticals, to pharmaceutical compositions containing one or more compounds of formula (I), and especially to their use as CXCR7 receptor modulators.
    Type: Grant
    Filed: June 21, 2013
    Date of Patent: August 30, 2016
    Assignee: ACTELION PHARMACEUTICALS LTD
    Inventors: Heinz Fretz, Markus Gude, Philippe Guerry, Thierry Kimmerlin, Francois Lehembre, Thomas Pfeifer, Anja Valdenaire
  • Patent number: 9428453
    Abstract: Cystine analogs that improve the solubility of L-cystine in urine for treatment of cystinuria and which have the structure: and pharmaceutically acceptable salts, solvates and prodrugs thereof, wherein each R and R? pair are independently selected from (i) or (ii); (i) R and R? are independently selected from hydrogen, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted alcohol, substituted or unsubstituted aryl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted heterocyclic, and substituted or unsubstituted heteroaryl, or (ii) R and R? together form a substituted or unsubstituted heterocyclic ring structure, or a substituted or unsubstituted heteroaryl ring structure; X is hydrogen, or an alkyl; and Y is O or S.
    Type: Grant
    Filed: January 2, 2014
    Date of Patent: August 30, 2016
    Assignee: RUTGERS, THE STATE UNIVERSITY OF NEW JERSEY
    Inventors: Longqin Hu, Amrik Sahota
  • Patent number: 9403775
    Abstract: The present invention provides a compound of Formula I or Formula II: enantiomer, diastereomer, prodrug, solvate, metabolite, or pharmaceutically acceptable salt thereof, wherein constituent variables are provided herein. The compounds of Formula I and II are modulators of metalloproteases and are useful in treating diseases associated with metalloprotease activity such as arthritis, cancer, cardiovascular disorders, skin disorders, inflammation and allergic conditions.
    Type: Grant
    Filed: November 27, 2013
    Date of Patent: August 2, 2016
    Assignees: Incyte Corporation, Incyte Holdings Corporation
    Inventors: Wenqing Yao, Jincong Zhuo, Meizhong Xu, Fenglei Zhang, Brian W. Metcalf
  • Patent number: 9402836
    Abstract: Herein are disclosed indoles of formula (I) where the various groups are defined herein, and which are useful for treating cancer.
    Type: Grant
    Filed: July 9, 2015
    Date of Patent: August 2, 2016
    Assignee: GlaxoSmithKline LLC
    Inventors: James Brackley, III, Joelle Lorraine Burgess, Seth Wilson Grant, Neil W. Johnson, Steven David Knight, Louis Vincent LaFrance, III, William Henry Miller, Kenneth Allen Newlander, Stuart Paul Romeril, Meagan B. Rouse, Xinrong Tian, Sharad Kumar Verma
  • Patent number: 9265738
    Abstract: Compounds and methods are provided for decreasing demyelinating inflammatory disease in a subject by inhibiting the activity of chemokine-like receptor 1 (CMKLR1). In some embodiments such methods include treating demyelinating inflammatory disease in a subject by administering an agent that antagonizes the activity of chemokine-like receptor 1 (CMKLR1) and/or a CMKLR1 ligand (e.g., chemerin or other endogenous CMKLR1 ligands). Candidate compounds include, without limitation, analogs and variants of 2-(alpha-naphthoyl)ethyltrimethylammonium iodide.
    Type: Grant
    Filed: January 15, 2013
    Date of Patent: February 23, 2016
    Assignee: The Board of Trustees of the Leland Stanford Junior University
    Inventors: Kareem Graham, Jian Zhang, Eugene C. Butcher, Brian A. Zabel
  • Patent number: 9242962
    Abstract: The present invention relates to a method of treating T cell mediated inflammatory immune diseases or T cell mediated hypersensitivity diseases, which comprises administering to a human in need thereof an effective amount of a compound which inhibits EZH2 and/or EZH1, or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: November 2, 2012
    Date of Patent: January 26, 2016
    Assignee: GlaxoSmithKline Intellectual Property (No. 2) Limited
    Inventors: Anna K. Bassil, Soren Beinke, Rabinder Kumar Prinjha
  • Patent number: 9227951
    Abstract: This invention provides compounds of formula (I): wherein X1, X2, X3, R2, R4b, R1, and G have values as described in the specification, useful as inhibitors of HDAC6. The invention also provides pharmaceutical compositions comprising the compounds of the invention and methods of using the compositions in the treatment of proliferative, inflammatory, infectious, neurological or cardiovascular diseases or disorders.
    Type: Grant
    Filed: September 12, 2013
    Date of Patent: January 5, 2016
    Assignee: Millennium Pharmaceuticals, Inc.
    Inventors: Christopher Blackburn, Kenneth M. Gigstad, He Xu
  • Patent number: 9198913
    Abstract: The present invention relates to novel nitroimidazooxazines, to their preparation, and to their use as drugs for treating Mycobacterium tuberculosis and other microbial infections, either alone or in combination with other anti-infective treatments.
    Type: Grant
    Filed: July 30, 2010
    Date of Patent: December 1, 2015
    Assignee: Global Alliance for TB Drug Development
    Inventors: William Alexander Denny, Andrew Mark Thompson, Adrian Blaser, Zhenkun Ma, Brian Desmond Palmer, Hamish Scott Sutherland, Iveta Kmentova
  • Patent number: 9150564
    Abstract: Certain substituted urea derivatives selectively modulate the cardiac sarcomere, for example by potentiating cardiac myosin, and are useful in the treatment of systolic heart failure including congestive heart failure.
    Type: Grant
    Filed: September 18, 2014
    Date of Patent: October 6, 2015
    Assignee: CYTOKINETICS, INC.
    Inventors: Bradley Paul Morgan, Alex Muci, Pu-Ping Lu, Erica Anne Kraynack, Todd Tochimoto, David J. Morgans, Jr.
  • Patent number: 9114141
    Abstract: Herein are disclosed indoles of formula (I) where the various groups are defined herein, and which are useful for treating cancer.
    Type: Grant
    Filed: January 23, 2015
    Date of Patent: August 25, 2015
    Assignee: GlaxoSmithKline LLC
    Inventors: William Henry Miller, Xinrong Tian, Shared Kumar Verma
  • Patent number: 9040539
    Abstract: A process for the preparation of a chiral compound, in particular posaconazole, wherein the process comprises mixing and reacting the compounds of formula (I) Y3—NH2; of formula (IIa) 0=C?N—Y0 and/or of formula (IIb) and of formula (III) in a solvent in any order to obtain a reaction mixture containing a chiral compound of formula (IV) and/or formula (V).
    Type: Grant
    Filed: May 18, 2011
    Date of Patent: May 26, 2015
    Assignee: SANDOZ AG
    Inventors: Michael Oberhuber, Joerg Salchenegger, Dominic De Souza, Martin Albert, Thorsten Wilhelm, Martin Langner, Hubert Sturm, Hans-Peter Spitzenstaetter
  • Patent number: 9035096
    Abstract: The invention relates to compounds represented by Structural Formula I, which can bind to CCR9 receptors and block the binding of a ligand (e.g., TECK) to the receptors. The invention also relates to a method of inhibiting a function of CCR9, and to the use compounds represented by Structural Formula I in research, therapeutic, prophylactic and diagnostic methods.
    Type: Grant
    Filed: October 9, 2013
    Date of Patent: May 19, 2015
    Assignee: Millennium Pharmaceuticals, Inc.
    Inventors: Paul E. Fleming, Geraldine C. B. Harriman, Zhan Shi, B. Shaowu Chen
  • Publication number: 20150133442
    Abstract: The invention features compositions and methods for inhibiting the Pin1 protein, and the treatment of disorders characterized by elevated Pin1 levels.
    Type: Application
    Filed: June 7, 2013
    Publication date: May 14, 2015
    Inventors: Kun Ping Lu, Matthew Brian Boxer, Mindy Irene Emily Davis, Rajan Pragani, Min Shen, Anton Momtchilov Simeonov, Shuo Wei, Xiao Zhen Zhou
  • Patent number: 9028874
    Abstract: The present invention is directed to multiple a-lipoic acid-containing hydrophobic compounds (mALAs) capable of acting as scavengers of free radicals, metals and reactive oxygen species (ROS). Methods of synthesizing novel antioxidant mALAs, spontaneous emulsification or nanoprecipitaion thereof to produce antioxidant nanospheres and their use in preventing or treating diseases or conditions caused by oxidative stress and other free radical mediated conditions are also described. Another aspect of this invention is the use of these antioxidant nanospheres for the preparation of antioxidant particulate delivery system of therapeutic agents.
    Type: Grant
    Filed: December 30, 2008
    Date of Patent: May 12, 2015
    Assignee: Cedars-Sinai Medical Center
    Inventors: John S. Yu, Bong Seop Lee
  • Publication number: 20150119383
    Abstract: Embodiments disclosed herein generally relate to acamprosate formulations, methods of use of the formulations, to methods of using the formulations in combination with at least one other medication, and to combination products and compositions comprising the formulations and at least one other medication, such as neuroleptic (antipsychotic) and/or antidepressant drugs.
    Type: Application
    Filed: June 5, 2014
    Publication date: April 30, 2015
    Inventors: Barry S. Fogel, William D. Kerns, Kei-Lai Fong, San-Laung Chow, Edward Lin, David Wong
  • Publication number: 20150105397
    Abstract: The present inventions relate to substituted piperazine derivatives of general formula (I) and to the manufacture of said compounds, pharmaceutical compositions comprising a compound according to general formula (I), and the use of said compounds for the treatment of various medical conditions related to glycine transporter-1 (GlyT1).
    Type: Application
    Filed: October 14, 2014
    Publication date: April 16, 2015
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: Christoph HOENKE, Riccardo GIOVANNINI, Uta LESSEL, Holger ROSENBROCK, Bernhard SCHMID
  • Publication number: 20150099747
    Abstract: The invention comprises reagents and methods for detecting cancer-associated mutations in the human EZH2 gene. Further, a method of detecting the mutations and a method of treatment are disclosed.
    Type: Application
    Filed: October 7, 2014
    Publication date: April 9, 2015
    Inventors: Xiaoju Max Ma, Chitra Manohar, Alison Tsan
  • Publication number: 20150086604
    Abstract: Biodegradable polymer-coated surgical meshes formed into pouches are described for use with cardiac rhythm management devices (CRMs) and other implantable medical devices. Such meshes are formed into a receptacle, e.g., a pouch or other covering, capable of encasing, surrounding and/or holding the cardiac rhythm management device or other implantable medical device for the purpose of securing it in position, inhibiting or reducing bacterial growth, providing pain relief and/or inhibiting scarring or fibrosis on or around the CRM or other implantable medical device. Preferred embodiments include surgical mesh pouches coated with one or more biodegradable polymers that can act as a stiffening agent by coating the filaments or fibers of the mesh to temporarily immobilize the contact points of those filaments or fibers and/or by increasing the stiffness of the mesh by at least 1.1 times its original stiffness.
    Type: Application
    Filed: September 23, 2013
    Publication date: March 26, 2015
    Inventors: Fatima Buevich, Frank Do, William McJames, Satish Pulapura, William Edelman, Arikha Moses, Mason Diamond, Shari Timothy
  • Patent number: 8987274
    Abstract: The present invention provides a compound of Formula (1): as described herein or a pharmaceutically acceptable salt or solvate thereof. The compounds are useful as inhibitors of the HDM2 protein. Also disclosed are pharmaceutical compositions comprising the above compounds and potential methods of treating cancer using the same.
    Type: Grant
    Filed: October 23, 2012
    Date of Patent: March 24, 2015
    Assignee: Merck Sharp & Dohme Corp
    Inventors: Latha G. Nair, Stephane L. Bogen, Ronald J. Doll, Yao Ma, Yuan Tian
  • Publication number: 20150051161
    Abstract: The present invention provides compositions and methods for detecting carboxymethyl-lysine (CML) and circulating receptor for advanced glycation end (RAGE) products, and methods for correlating CML and RAGE levels with age-related disease. In particular, serum CML and/or circulating receptor for advanced glycation end (RAGE) products can be used as a clinical biomarker in diagnostics to identify people who are at a higher risk of developing adverse ageing-related outcomes.
    Type: Application
    Filed: April 10, 2014
    Publication date: February 19, 2015
    Applicant: THE JOHNS HOPKINS UNIVERSITY
    Inventors: Richard David Semba, Luigi Ferruci, Edward G. Lakatta
  • Publication number: 20150051194
    Abstract: 8-Substituted-2,6-methano-3-benzazocines of general structure are useful as analgesics, anti-diarrheal agents, anticonvulsants, antitussives and anti-addiction medications.
    Type: Application
    Filed: October 31, 2014
    Publication date: February 19, 2015
    Applicant: RENSSELAER POLYTECHNIC INSTITUTE
    Inventor: Mark P. WENTLAND
  • Publication number: 20150051220
    Abstract: A compound of formula (I) for use in the treatment of a condition or disorder associated with nicotinamide adenine dinucleotide phosphate oxidase.
    Type: Application
    Filed: March 14, 2013
    Publication date: February 19, 2015
    Applicant: GLUCOX BIOTECH AB
    Inventors: Mona Wilcke, Erik Walum, Per Wikstrom
  • Patent number: 8957070
    Abstract: The present invention provides a glucokinase activator containing a compound represented by the formula (I): wherein each symbol is as defined in the specification, or a salt thereof or a prodrug thereof. According to the present invention, a glucokinase activator useful as a pharmaceutical agent such as agent for the prophylaxis or treatment of diabetes, obesity and the like, and the like can be provided.
    Type: Grant
    Filed: April 20, 2006
    Date of Patent: February 17, 2015
    Assignee: Takeda Pharmaceutical Company Limited
    Inventors: Tsuneo Yasuma, Osamu Ujikawa
  • Publication number: 20150005275
    Abstract: The present invention discloses compounds according to Formula I: wherein R1, R2, R3, L, and the subscript m are as defined herein. The present invention relates to compounds and their use in the treatment of cystic fibrosis, methods for their production, pharmaceutical compositions, and methods of treatment using the same, for the treatment of cystic fibrosis by administering a compound of the invention.
    Type: Application
    Filed: May 6, 2014
    Publication date: January 1, 2015
    Inventors: Steven Emiel Van der Plas, Oscar Mammoliti, Christel Jeanne Marie Menet, Giovanni Alessandro Tricarico, Ann De De Blieck, Caroline Martine Andrée Marie Joannesse, Hans Kelgtermans, Tom Roger Lisette De Munck
  • Patent number: 8916161
    Abstract: The present invention provides a method of treating BPH using modified pore-forming proteins (MPPs). These MPPs are derived from naturally occurring cytotoxic proteins (nPPs) that kill cells by forming pores or channels in the cell membrane, resulting in cell death. The MPPs are generated by modification of the nPPs such that they are capable of being selectively activated at normal prostate cells. Such modification may include the addition of a prostate-specific protease cleavage site to the activation sequence, and/or the addition of a prostate-specific targeting domain to allow selective targeting of prostate cells. These MPPs are capable of selectively targeting and killing normal prostate cells in vivo. The MPPs may be used either alone or in combination with other therapies for the treatment of BPH.
    Type: Grant
    Filed: June 14, 2006
    Date of Patent: December 23, 2014
    Assignee: Sophiris Bio Inc.
    Inventor: James Thomas Buckley
  • Publication number: 20140356360
    Abstract: The present invention relates to piperazinyl derivatives of formula (I) and the use thereof as a drug, particularly for the treatment of cancer, the pharmaceutical compositions containing said derivatives, and the method for synthesising same.
    Type: Application
    Filed: December 28, 2012
    Publication date: December 4, 2014
    Inventor: Marc-Henry PITTY
  • Patent number: 8901115
    Abstract: The present invention provides compounds of Formula (Ia): or stereoisomers, tautomers, or pharmaceutically acceptable salts thereof, wherein all the variables are as defined herein. These compounds are selective factor XIa inhibitors or dual inhibitors of FXIa and plasma kallikrein. This invention also relates to pharmaceutical compositions comprising these compounds and methods of treating thromboembolic and/or inflammatory disorders using the same.
    Type: Grant
    Filed: August 6, 2012
    Date of Patent: December 2, 2014
    Assignee: Bristol-Myers Squibb Company
    Inventors: Patrick Y. S. Lam, Charles G. Clark, James R. Corte, William R. Ewing, Paul J. Gilligan, Yoon Jeon, Wu Yang, Leon M. Smith, II, Yufeng Wang
  • Publication number: 20140350000
    Abstract: This document provides methods and materials related to genetic markers for predicting response to a treatment for schizophrenia (SZ). For example, methods for using such genetic markers to select optimal treatments are provided.
    Type: Application
    Filed: August 13, 2014
    Publication date: November 27, 2014
    Inventors: Mark David Brennan, Timothy Lynn Ramsey
  • Patent number: 8883790
    Abstract: The invention provides combinations comprising (or consisting essentially of) one or more ancillary compound(s) and a compound of the formula (I): or salts, tautomers, solvates and N-oxides thereof; wherein R1 is hydroxy or hydrogen; R2 is hydroxy; methoxy or hydrogen; provided that at least one of R1 and R2 is hydroxy; R3 is selected from hydrogen; halogen; cyano; optionally substituted C1-5 hydrocarbyl and optionally substituted C1-5 hydrocarbyloxy; R4 is selected from hydrogen; a group —(O)n—R7 where n is 0 or 1 and R7 is an optionally substituted acyclic C1-5 hydrocarbyl group or a monocyclic carbocyclic or heterocyclic group having 3 to 7 ring members; halogen; cyano; hydroxy; amino; and optionally substituted mono- or di-C1-5 hydrocarbyl-amino; or R3 and R4 together form a monocyclic carbocyclic or heterocyclic ring of 5 to 7 ring members; and NR5R6 forms an optionally substituted bicyclic heterocyclic group having 8 to 12 ring members of which up to 5 ring members are heteroatoms selected from oxyg
    Type: Grant
    Filed: October 12, 2007
    Date of Patent: November 11, 2014
    Assignee: Astex Therapeutics Limited
    Inventors: Neil James Gallagher, John Francis Lyons, Neil Thomas Thompson, Stephen Murray Yule, Christopher William Murray
  • Publication number: 20140329802
    Abstract: The purpose is to provide a compound which has an intestinal phosphate transporter (NPT-IIb) inhibitory action and is useful as an active ingredient of an agent for treating and/or preventing hyperphosphatemia. A tetrahydrobenzothiophene compound of the following formula (I) has NPT-IIb inhibitory action and can be used as an agent for treating and/or preventing hyperphosphatemia: wherein, R1 represents —O-lower alkyl, -lower alkylene-phenyl, or the like; R2 and R3 are the same as or different from each other and represent H, lower alkyl, cycloalkyl, aryl, heteroaryl or the like, or, R2 and R3 may be combined with a nitrogen atom to which they bind to form 5- to 7-membered saturated cyclic amino; R4's are the same as or different from each other and represent halogen, lower alkyl; and n represents 0 to 2.
    Type: Application
    Filed: March 28, 2014
    Publication date: November 6, 2014
    Applicant: Astellas Pharma Inc.
    Inventors: Shunichiro HACHIYA, Masanori Miura, Yoshimasa Imamura, Daisuke Kaga, Ippei Sato, Hiroyuki Moritomo, Koji Kato, Kazuhiro Terai, Yoh Terada
  • Patent number: 8871769
    Abstract: Certain substituted urea derivatives selectively modulate the cardiac sarcomere, for example by potentiating cardiac myosin, and are useful in the treatment of systolic heart failure including congestive heart failure.
    Type: Grant
    Filed: July 19, 2013
    Date of Patent: October 28, 2014
    Assignee: Cytokinetics, Inc.
    Inventors: Bradley Paul Morgan, Alex Muci, Pu-Ping Lu, Erica Anne Kraynack, Todd Tochimoto, David J. Morgans
  • Patent number: 8871753
    Abstract: The present invention relates to macrocyclic compounds of Formula I: or pharmaceutically acceptable salts thereof or quaternary ammonium salts thereof wherein constituent members are provided hereinwith, as well as their compositions and methods of use, which are JAK/ALK inhibitors useful in the treatment of JAK/ALK-associated diseases including, for example, inflammatory and autoimmune disorders, as well as cancer.
    Type: Grant
    Filed: April 23, 2009
    Date of Patent: October 28, 2014
    Assignee: Incyte Corporation
    Inventors: Andrew Paul Combs, Richard B. Sparks, Eddy W. Yue, Hao Feng, Michael Jason Bower, Wenyu Zhu
  • Patent number: RE47428
    Abstract: Agents for modulating methyl modifying enzymes, compositions and uses thereof are provided herein.
    Type: Grant
    Filed: January 24, 2018
    Date of Patent: June 11, 2019
    Assignee: Constellation Pharmaceuticals, Inc.
    Inventors: Brian K. Albrecht, James Edmund Audia, Les A. Dakin, Victor S. Gehling, Jean-Christophe Harmange, Christopher G. Nasveschuk, Rishi G. Vaswani