Additional Hetero Ring Other Than The Six-membered Hetero Rings Patents (Class 514/333)
  • Patent number: 11628163
    Abstract: The present description relates to 1-piperidinepropionic acid or pharmaceutically acceptable salts thereof, or pharmaceutical compositions comprising it, for use in the treatment of chronic fibrosing diseases.
    Type: Grant
    Filed: March 9, 2018
    Date of Patent: April 18, 2023
    Assignee: Università degli Studi di Padova
    Inventors: Patrizia Pontisso, Alessandra Biasiolo, Andrea Cappon, Andrea Martini, Santina Quarta, Mariagrazia Ruvoletto, Cristian Turato, Gianmarco Villano
  • Patent number: 11591328
    Abstract: The present invention relates to a CSF1R inhibitor, and in particular to a highly active CSF1R inhibitor compound having the structure of formula (I). Said compound of the present invention has high inhibitory activity on CSF1R.
    Type: Grant
    Filed: May 24, 2019
    Date of Patent: February 28, 2023
    Assignee: XIAMEN BIOTIME BIOTECHNOLOGY CO., LTD.
    Inventors: Shifeng Liu, Zhiyong Yu, Wei Pang, Ji Wang, Peng Chen
  • Patent number: 11434234
    Abstract: The present invention provides compounds having the general structural formula (I) and pharmaceutically acceptable derivatives thereof, as described generally and in classes and subclasses herein, and additionally provides pharmaceutical compositions thereof, and methods for the use thereof for the treatment of any of a number of conditions or diseases involving elevated levels of aldosterone or abnormal or excessive fibrosis, such as kidney disease and hypertension.
    Type: Grant
    Filed: November 23, 2020
    Date of Patent: September 6, 2022
    Assignee: Angion Biomedica Corp.
    Inventors: Bijoy Panicker, Lambertus J. W. M. Oehlen
  • Patent number: 11419858
    Abstract: The present disclosure relates generally to compositions and methods for treating, preventing, or slowing the rate of development of a disease or condition mediated by a nonsense mutation in the bone morphogenetic protein receptor type II (Bmpr2) in a subject in need thereof. The method entails administering to the subject a compound of the present disclosure, such as GJ103 and a salt thereof.
    Type: Grant
    Filed: February 25, 2020
    Date of Patent: August 23, 2022
    Assignee: Lundquist Institute for Biomedical Innovation at Harbor-UCLA Medical Center
    Inventors: Virender K. Rehan, Terence M. Doherty
  • Patent number: 11304917
    Abstract: A method of treating tinnitus in a subject is described that includes administering a therapeutically effective amount of a group II metabotropic glutamate receptor (mGluR) agonist to the subject. A method of screening a subject having tinnitus for treatment with a group II mGluR agonist that includes testing the use of residual inhibition to suppress tinnitus in the subject, wherein suppression of tinnitus by residual inhibition indicates that a group II mGluR agonist would be effective for treating tinnitus in the subject, is also described.
    Type: Grant
    Filed: February 19, 2016
    Date of Patent: April 19, 2022
    Assignee: NORTHEAST OHIO MEDICAL UNIVERSITY
    Inventor: Alexander V. Galazyuk
  • Patent number: 11230537
    Abstract: The invention provides new polymorphs of N-[(3-fluoro-4-methoxypyridin-2-yl)methyl]-3-(methoxymethyl)-1-({4-[(2-oxopyridin-1-yl)methyl]phenyl}methyl)pyrazole-4-carboxamide and salts thereof, pharmaceutical compositions containing them and their use as kallikrein inhibitors in therapy.
    Type: Grant
    Filed: June 1, 2017
    Date of Patent: January 25, 2022
    Assignee: KalVista Pharmaceuticals Limited
    Inventors: Haydn Beaton, David Malcolm Crowe, Hannah Joy Edwards, Nicholas James Griffiths-Haynes
  • Patent number: 11225472
    Abstract: The present invention relates to the compounds according to Formula (I), the racemates, enantiomers, diastereomers thereof or pharmaceutical acceptable salts thereof, or pharmaceutical compositions comprising these, for the treatment or prevention of metabolic disorders. The compounds according to Formula (I) are, as GPR40 agonists, available for oral administration with glucose-dependent insulin secretion mechanism, which exhibit excellent glucose lowering efficacy without the risk of hypoglycemia. Thus, the compounds and/or pharmaceutical compositions comprising the compounds as effective components are useful in treating and/or preventing symptoms of type 2 diabetes through adequate control of blood glucose.
    Type: Grant
    Filed: December 14, 2017
    Date of Patent: January 18, 2022
    Inventors: Jae-Hoon Kang, Hong-Sub Lee, Kyung-Mi An, Chang-Hee Hong, Hyun-Jung Kwak, Shuo-Lin Cui, Hyo-Jung Song
  • Patent number: 11078194
    Abstract: Disclosed in the present invention are a salt form and a crystal form serving as FGFR and VEGFR inhibitor compounds, a preparation method therefor, and medical uses thereof.
    Type: Grant
    Filed: December 7, 2018
    Date of Patent: August 3, 2021
    Assignee: HARBIN ZHENBAO PHARMACEUTICAL CO., LTD.
    Inventors: Zhengxia Chen, Yang Zhang, Meibi Dai, Hongfei Cheng, Suqin Yang, Wenju Li, Jian Li, Shuhui Chen
  • Patent number: 11066360
    Abstract: Disclosed are compounds of formula I, and pharmaceutically acceptable salts thereof. The compounds are inhibitors of plasma kallikrein. Also provided are pharmaceutical compositions comprising at least one compound of the invention, and methods involving use of the compounds and compositions of the invention in the treatment and prevention of diseases and conditions characterized by unwanted plasma kallikrein activity.
    Type: Grant
    Filed: December 18, 2019
    Date of Patent: July 20, 2021
    Assignee: BioCryst Pharmaceuticals, Inc.
    Inventors: Pravin L. Kotian, Yarlagadda S. Babu, V. Satish Kumar, Weihe Zhang, Lakshminarayana Vogeti
  • Patent number: 11033537
    Abstract: The present invention provides, inter alia, a composition containing a compound of formula (I): or a pharmaceutically acceptable salt thereof, optionally, in combination with at least one immune checkpoint inhibitor compound. Kits containing the composition, and methods of using the composition for ameliorating or treating the effects of a disease such as a cancer, in a subject, are also provided herein.
    Type: Grant
    Filed: June 29, 2020
    Date of Patent: June 15, 2021
    Assignee: BIOMED VALLEY DISCOVERIES, INC.
    Inventors: Saurabh Saha, Linping Zhang, Xiaoyan Michelle Zhang
  • Patent number: 11017787
    Abstract: An apparatus to accentuate a fundamental frequency of a singer's utterance. The apparatus includes a frequency discriminator configured to detect the fundamental frequency of the singer's utterance. The apparatus also includes a device configured to process the singer's utterance, the device comprising at least one of: a filter connected to the frequency discriminator and configured to isolate the fundamental frequency; or a synthesizer connected to the filter and configured to isolate the fundamental frequency. The apparatus also includes a speaker configured to emit an audio signal that effectively reproduces and accentuates the fundamental frequency back to the singer.
    Type: Grant
    Filed: February 8, 2019
    Date of Patent: May 25, 2021
    Assignee: Board of Regents, The University of Texas System
    Inventor: Eric A. Freudenthal
  • Patent number: 10980788
    Abstract: Provided are methods and compositions for treating cancers in patients carrying an IDH1 mutation using an inhibitor of a mutant IDH1 enzyme.
    Type: Grant
    Filed: June 7, 2019
    Date of Patent: April 20, 2021
    Assignee: Agios Pharmaceuticals, Inc.
    Inventor: Samuel V. Agresta
  • Patent number: 10851065
    Abstract: Disclosed herein are compounds, or pharmaceutically acceptable salts thereof, and methods of using the compounds for treating breast cancer by administration to a subject in need thereof a therapeutically effective amount of the compounds or pharmaceutically acceptable salts thereof. The breast cancer may be an ER-positive breast cancer and/or the subject in need of treatment may express a mutant ER-? protein.
    Type: Grant
    Filed: September 22, 2017
    Date of Patent: December 1, 2020
    Assignee: Eisai R&D Management Co., Ltd.
    Inventors: Mark Bock, Ming-Hong Hao, Manav Korpal, Vijay Kumar Nyavanandi, Xiaoling Puyang, Susanta Samajdar, Peter Gerard Smith, John Wang, Guo Zhu Zheng, Ping Zhu
  • Patent number: 10807975
    Abstract: The present inventors discovered that the molecule pyridinylthiazolamine (PTA) specifically prevents the protein-protein interaction of hLC3 with hAtg3 in vitro and in cell based assays. The inventors have developed a novel class of PTA analogs which also prevents the protein-protein interaction of hLC3 with hAtg3 in vitro, and in cell based assays, and which can be used in prior to, or in combination with chemotherapeutic agents to treat proliferative diseases such as cancer.
    Type: Grant
    Filed: August 28, 2018
    Date of Patent: October 20, 2020
    Assignee: The Johns Hopkins University
    Inventor: Jurgen Bosch
  • Patent number: 10787442
    Abstract: Provided are IDO inhibitor compounds of Formula I and pharmaceutically acceptable salts thereof, their pharmaceutical compositions, their methods of preparation, and methods for their use in the prevention and/or treatment of diseases.
    Type: Grant
    Filed: December 15, 2017
    Date of Patent: September 29, 2020
    Assignee: GLAXOSMITHKLINE INTELLECTUAL PROPERTY DEVELOPMENT LIMITED
    Inventors: John G. Catalano, Martha Alicia De La Rosa, Wieslaw Mieczyslaw Kazmierski, Vicente Samano
  • Patent number: 10716782
    Abstract: The present invention provides, inter alia, a composition containing a compound of formula (I): or a pharmaceutically acceptable salt thereof, optionally, in combination with at least one immune checkpoint inhibitor compound. Kits containing the composition, and methods of using the composition for ameliorating or treating the effects of a disease such as a cancer, in a subject, are also provided herein.
    Type: Grant
    Filed: November 22, 2019
    Date of Patent: July 21, 2020
    Assignee: BIOMED VALLEY DISCOVERIES, INC.
    Inventors: Saurabh Saha, Linping Zhang, Xiaoyan Michelle Zhang
  • Patent number: 10668048
    Abstract: Antibacterial small molecule compounds, termed liptins, bind to phosphatidylglycerol in bacterial plasma membranes. The small molecule compounds comprise a three-dimensional complementary binding pocket for phosphatidylglycerol, disrupting membrane function in a bacteriostatic or bactericidal manner. Methods of inhibiting bacterial growth and/or treating Gram-positive or Gram-negative bacterial infection using such compounds are also disclosed.
    Type: Grant
    Filed: July 27, 2018
    Date of Patent: June 2, 2020
    Assignee: Wichita State University
    Inventors: Dennis H. Burns, Douglas S. English
  • Patent number: 10604515
    Abstract: The invention discloses compounds of Formula I, wherein X1, X2, R1, and R2 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 comprising the same, and methods of treating cystic fibrosis by administering a compound of the invention.
    Type: Grant
    Filed: October 19, 2018
    Date of Patent: March 31, 2020
    Assignees: AbbVie S.á.r.l., Galapagos NV
    Inventors: Robert J. Altenbach, Andrew Bogdan, Ghjuvanni Petru Diunisu Coti, Marlon D. Cowart, Stephen N. Greszler, Hans Kelgtermans, Philip R. Kym, Steven Emiel Van der Plas, Xueqing Wang
  • Patent number: 10556801
    Abstract: The present invention relates to a method for the preparation of a treated zeolitic material having a BEA framework structure including the steps of: (i) providing a zeolitic material having a BEA framework structure, wherein the BEA framework structure includes YO2 and X2O3, wherein Y is a tetravalent element, and X is a trivalent element, and wherein the zeolitic material having a BEA framework structure is obtainable and/or obtained from an organotemplate-free synthetic process; (ii) calcining the zeolitic material provided in step (i) at a temperature of 650° C. or more; and (iii) treating the calcined zeolitic material obtained from step (ii) with an aqueous solution having a pH of 5 or less, as well as to zeolitic materials per se preferably obtainable according to the inventive method and to their use, and to a process for converting oxygenates to olefins employing the inventive zeolitic materials.
    Type: Grant
    Filed: February 11, 2016
    Date of Patent: February 11, 2020
    Assignee: BASF SE
    Inventors: Mathias Feyen, Stefan Maurer, Ulrich Mueller, Xinhe Bao, Weiping Zhang, Dirk de Vos, Hermann Gies, Feng-Shou Xiao, Yokoi Toshiyuki, Bilge Yilmaz, Ryoichi Otomo
  • Patent number: 10485796
    Abstract: The present invention provides, inter alia, a composition containing a compound of formula (I): or a pharmaceutically acceptable salt thereof, optionally, in combination with at least one immune checkpoint inhibitor compound. Kits containing the composition, and methods of using the composition for ameliorating or treating the effects of a disease such as a cancer, in a subject, are also provided herein.
    Type: Grant
    Filed: November 10, 2017
    Date of Patent: November 26, 2019
    Assignee: BIOMED VALLEY DISCOVERIES, INC.
    Inventors: Saurabh Saha, Linping Zhang, Xiaoyan Michelle Zhang
  • Patent number: 10316020
    Abstract: The present invention provides a compound of formula (I) or a pharmaceutically acceptable salt thereof; a method for manufacturing the compounds of the invention, and its therapeutic uses. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.
    Type: Grant
    Filed: December 16, 2016
    Date of Patent: June 11, 2019
    Assignee: Novartis AG
    Inventors: Christopher Adams, Takeru Ehara
  • Patent number: 10307427
    Abstract: The present invention relates to compounds of Formula (I): Wherein variables are as defined above. The compounds have apoptosis signal-regulating kinase (“ASK”) inhibitory activity, and are thus useful in the treatment of ASK1-mediated conditions, including autoimmune disorders, inflammatory diseases, cardiovascular diseases, diabetes, diabetic nephropathy, cardio-renal diseases, including kidney disease, fibrotic diseases, respiratory diseases, COPD, idiopathic pulmonary fibrosis, acute lung injury, acute and chronic liver diseases, and neurodegenerative diseases.
    Type: Grant
    Filed: March 21, 2018
    Date of Patent: June 4, 2019
    Assignee: Gilead Sciences, Inc.
    Inventor: Gregory Notte
  • Patent number: 10308629
    Abstract: Compounds of formula (I) as described herein, processes for their production and their use as pharmaceuticals.
    Type: Grant
    Filed: August 1, 2016
    Date of Patent: June 4, 2019
    Assignee: BAYER PHARMA AKTIENGESELLSCHAFT
    Inventors: Keith Graham, Ulrich Klar, Hans Briem, Gerhard Siemeister, Ursula Mönning
  • Patent number: 10155763
    Abstract: The present invention provides a novel 2-pyridyl substituted imidazole derivative, or a pharmaceutically acceptable salt or solvate thereof, which selectively inhibits the transforming growth factor-? (TGF-?) type I receptor (ALK5) and/or the activin type I receptor (ALK4); a pharmaceutical composition comprising same as an active ingredient; and a use of the 2-pyridyl substituted imidazole derivative for the manufacture of a medicament for preventing or treating a disease mediated by ALK5 and/or ALK4 receptors in a mammal.
    Type: Grant
    Filed: July 13, 2012
    Date of Patent: December 18, 2018
    Assignee: TIUMBIO CO., LTD.
    Inventors: Ju Young Lee, Keun-Ho Ryu, Jae-Sun Kim, Yong-Hyuk Kim, Dong-Chul Shin, Bong-yong Lee, Sang-hwan Kang, Hyun-Jung Lee, Hoechul Jung, Young Ah Shin, Euisun Park, Jaeseung Ahn, Hun-Taek Kim, Je Ho Ryu
  • Patent number: 10138227
    Abstract: The invention discloses compounds of Formula I, wherein X1, X2, R1, and R2 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 comprising the same, and methods of treating cystic fibrosis by administering a compound of the invention.
    Type: Grant
    Filed: May 23, 2017
    Date of Patent: November 27, 2018
    Assignees: AbbVie S.á.r.l., Galapagos NV
    Inventors: Robert J. Altenbach, Andrew Bogdan, Ghjuvanni Petru Diunisu Coti, Marlon D. Cowart, Stephen N Greszler, Hans Kelgtermans, Philip R Kym, Steven Emiel Van der Plas, Xueqing Wang
  • Patent number: 9861621
    Abstract: The present invention provides, inter alia, a composition containing a compound of formula (I): or a pharmaceutically acceptable salt thereof, optionally, in combination with at least one immune checkpoint inhibitor compound. Kits containing the composition, and methods of using the composition for ameliorating or treating the effects of a disease such as a cancer, in a subject, are also provided herein.
    Type: Grant
    Filed: June 28, 2016
    Date of Patent: January 9, 2018
    Assignee: Biomed Valley Discoveries, Inc.
    Inventors: Saurabh Saha, Linping Zhang, Xiaoyan Michelle Zhang
  • Patent number: 9796683
    Abstract: Disclosed herein are compounds, or pharmaceutically acceptable salts thereof, and methods of using the compounds for treating breast cancer by administration to a subject in need thereof a therapeutically effective amount of the compounds or pharmaceutically acceptable salts thereof. The breast cancer may be an ER-positive breast cancer and/or the subject in need of treatment may express a mutant ER-? protein.
    Type: Grant
    Filed: May 27, 2016
    Date of Patent: October 24, 2017
    Assignee: Eisai R&D Management Co., Ltd.
    Inventors: Mark Bock, Ming-Hong Hao, Manav Korpal, Vijay Kumar Nyavanandi, Xiaoling Puyang, Susanta Samajdar, Peter Gerard Smith, John Wang, Guo Zhu Zheng, Ping Zhu
  • Patent number: 9782404
    Abstract: Methods for treatment of disease-induced ataxia and non-ataxic imbalance are disclosed. The methods involve treating a patient with a compound having nicotinic acetylcholine receptor activity.
    Type: Grant
    Filed: August 29, 2014
    Date of Patent: October 10, 2017
    Assignee: UNIVERSITY OF SOUTH FLORIDA
    Inventors: Theresa A. Zesiewicz, Kelly L. Sullivan
  • Patent number: 9763925
    Abstract: Disclosed are compounds of formula (I): which are of use in the treatment of bacterial diseases and infections, to compositions containing those compounds and to methods of treating bacterial diseases and infections using the compounds. In particular, the compounds are useful for the treatment of infection with, and diseases caused by, Clostridium difficile.
    Type: Grant
    Filed: March 8, 2016
    Date of Patent: September 19, 2017
    Assignee: SUMMIT THERAPEUTICS PLC
    Inventors: Francis Xavier Wilson, Peter David Johnson, Richard Vickers, Richard Storer, Graham Michael Wynne, Alan Geoffrey Roach, Olivier De Moor, Colin Richard Dorgan, Paul James Davis
  • Patent number: 9751854
    Abstract: The present invention provides a compound of formula I: and pharmaceutically acceptable salts thereof, wherein X, R1, R2, R3, R4, R5, L1, L2, m, and n, are as described in the specification. Such compounds are inhibitors of VPS34 and thus useful for treating proliferative, inflammatory, or cardiovascular disorders.
    Type: Grant
    Filed: November 9, 2016
    Date of Patent: September 5, 2017
    Assignee: Millennium Pharmaceuticals, Inc.
    Inventors: Indu T. Bharathan, Chris Blackburn, Jeffrey P. Ciavarri, Jouhara Chouitar, Courtney A. Cullis, Natalie D'Amore, Paul E. Fleming, Kenneth M. Gigstad, Krista E. Gipson, Mario Girard, Yongbo Hu, Janice Lee, Gang Li, Mansoureh Rezaei, Michael D. Sintchak, Francois Soucy, Stephen G. Stroud, Tricia J. Vos, Tzu-Tshin Wong, He Xu, Tianlin Xu, Yingchun Ye
  • Patent number: 9725440
    Abstract: Compounds of the present invention, and pharmaceutically acceptable compositions thereof, are useful as modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator (“CFTR”). The present invention also relates to methods of treating CFTR mediated diseases using compounds of the present invention.
    Type: Grant
    Filed: February 27, 2015
    Date of Patent: August 8, 2017
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: Sara Hadida-Ruah, Mark Miller, Brian Bear, Jinglan Zhou, Jason McCartney, Peter Grootenhuis
  • Patent number: 9695147
    Abstract: The present invention provides intermediates useful for the synthesis of Perampanel and processes employing said intermediates for preparing Perampanel. The invention also provides processes for making the intermediates, crystalline forms of the intermediates and the use of the crystalline forms for preparing Perampanel.
    Type: Grant
    Filed: July 24, 2014
    Date of Patent: July 4, 2017
    Assignee: TEVA PHARMACEUTICALS INTERNATIONAL GMBH
    Inventor: Marian Buchlovic
  • Patent number: 9643934
    Abstract: A method for preparing a compound of formula k or a salt or solvate thereof, wherein R1 is as defined herein, the method comprising treating a compound of formula j or a salt or solvate thereof, with ammonia, to form the compound of formula k.
    Type: Grant
    Filed: October 14, 2013
    Date of Patent: May 9, 2017
    Assignee: Roche Palo Alto LLC
    Inventors: Charles Alois Dvorak, Keena Lynn Green, Gary R. Lee
  • Patent number: 9463190
    Abstract: Methods for treatment of disease-induced ataxia and non-ataxic imbalance are disclosed. The methods involve treating a patient with a compound having nicotinic acetylcholine receptor activity.
    Type: Grant
    Filed: March 31, 2009
    Date of Patent: October 11, 2016
    Assignee: UNIVERSITY OF SOUTH FLORIDA
    Inventors: Theresa A. Zesiewicz, Kelly L. Sullivan
  • Patent number: 9382228
    Abstract: Described are compounds of Formula I which find utility in the treatment of cancer, autoimmune diseases and metabolic bone disorders through inhibition of c-FMS (CSF-1R), c-KIT, and/or PDGFR kinases. These compounds also find utility in the treatment of other mammalian diseases mediated by c-FMS, c-KIT, or PDGFR kinases.
    Type: Grant
    Filed: March 14, 2014
    Date of Patent: July 5, 2016
    Assignee: Deciphera Pharmaceuticals, LLC
    Inventors: Daniel L. Flynn, Timothy Malcolm Caldwell, Michael D. Kaufman, William C. Patt, Thiwanka Samarakoon, Lakshminarayana Vogeti, Karen M. Yates
  • Patent number: 9326975
    Abstract: The present invention provides novel substituted pyrazolone compounds, pharmaceutical acceptable salts and formulations thereof useful in modulating the protein tyrosine kinase activity, and in modulating cellular activities such as proliferation, differentiation, apoptosis, migration and invasion. The invention also provides pharmaceutically acceptable compositions comprising such compounds and methods of using the compositions in the treatment of hyperproliferative disorders in mammals, especially humans.
    Type: Grant
    Filed: January 20, 2015
    Date of Patent: May 3, 2016
    Assignees: SUNSHINE LAKE PHARMA CO., LTD, CALITOR SCIENCES, LLC
    Inventors: Ning Xi, Yanjun Wu, Min Liao, Yanming Feng
  • Patent number: 9309224
    Abstract: Described are compounds of Formula 1 which find utility in the treatment of cancer, autoimmune diseases and metabolic bone disorders through inhibition of c-FMS (CSF-1R), c-KIT, and/or PDGFR kinases. These compounds also find utility in the treatment of other mammalian diseases mediated by c-FMS, c-KIT, or PDGFR kinases.
    Type: Grant
    Filed: March 14, 2014
    Date of Patent: April 12, 2016
    Assignee: Deciphera Pharmaceuticals, LLC.
    Inventors: Daniel L. Flynn, Timothy Malcolm Caldwell, Thiwanka Samarakoon, Lakshminarayana Vogeti, Michael D. Kaufman, William C. Patt, YuMi Ahn
  • Patent number: 9301953
    Abstract: A compound of formula: where Ar1, Ar2, X, R3, and m are as disclosed herein or a pharmaceutically acceptable salt thereof (a “Cycloheteroalkenyl Compound”); compositions comprising an effective amount of a Cycloheteroalkenyl Compound; and methods for treating or preventing pain, UI, an ulcer, IBD, IBS, an addictive disorder, Parkinson's disease, parkinsonism, anxiety, epilepsy, stroke, a seizure, a pruritic condition, psychosis, a cognitive disorder, a memory deficit, restricted brain function, Huntington's chorea, amyotrophic lateral sclerosis, dementia, retinopathy, a muscle spasm, a migraine, vomiting, dyskinesia, or depression in an animal comprising administering to an animal in need thereof an effective amount of a Cycloheteroalkenyl Compound are disclosed herein.
    Type: Grant
    Filed: December 17, 2013
    Date of Patent: April 5, 2016
    Assignee: Purdue Pharma L.P.
    Inventors: Qun Sun, Kate Xin Wen
  • Patent number: 9289467
    Abstract: A method of treating a degenerative bone condition of a subject includes administering to hematopoietic progenitor cells or osteoclast progenitor cells of the subject at least one agent that substantially reduces the interaction of at least one of C3a or C5a with the C3a receptor (C3aR) and/or C5a receptor (C5aR), a STAT3/IL-6 signaling pathway antagonist, and a combination thereof, the agent being administered to the hematopoietic progenitor cells or osteoclast progenitor cells at an amount effective to inhibit osteoclast differentiation of hematopoietic progenitor cells or osteoclast progenitor cells.
    Type: Grant
    Filed: August 10, 2012
    Date of Patent: March 22, 2016
    Assignee: Case Western Reserve University
    Inventors: Feng Lin, James E. Dennis, Zhidan Tu
  • Patent number: 9145373
    Abstract: Certain chemical entities are provided herein. Also provided are pharmaceutical compositions comprising at least one chemical entity and one or more pharmaceutically acceptable vehicle. Methods of treating patients suffering from certain diseases and disorders responsive to the inhibition of KMO activity are described, which comprise administering to such patients an amount of at least one chemical entity effective to reduce signs or symptoms of the disease or disorder are disclosed. These diseases include neurodegenerative disorders such as Huntington's disease. Also described are methods of treatment include administering at least one chemical entity as a single active agent or administering at least one chemical entity in combination with one or more other therapeutic agents. Also provided are methods for screening compounds capable of inhibiting KMO activity.
    Type: Grant
    Filed: August 9, 2013
    Date of Patent: September 29, 2015
    Assignee: CHDI FOUNDATION, INC.
    Inventors: John Wityak, Leticia M. Toledo-Sherman, Celia Dominguez, Stephen Martin Courtney, Christopher John Yarnold, Paula C. De Aguiar Pena, Andreas Scheel, Dirk Winkler
  • Patent number: 9120785
    Abstract: The present invention provides novel pyrimidine amines of formula I which are potent inhibitors of spleen tyrosine kinase, and are useful in the treatment and prevention of diseases mediated by said enzyme, such as asthma, COPD, rheumatoid arthritis, and cancer.
    Type: Grant
    Filed: May 4, 2012
    Date of Patent: September 1, 2015
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Michael D. Altman, Maria Emilia Di Francesco, Andrew M. Haidle, Ryan D. Otte, John Michael Ellis, Kaleen Konrad Childers, Alan B. Northrup, Liping Wang
  • Patent number: 9062032
    Abstract: [Problem] To provide a compound that 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. [Means for Solution] The present inventors conducted their studies on a compound that has an NPT-IIb inhibitory action and is useful as an active ingredient of an agent for treating and/or preventing hyperphosphatemia. As a result, they created an aminoalkyl-substituted N-thienylbenzamide derivative which has NPT-IIb inhibitory action, thereby completing the present invention. The aminoalkyl-substituted N-thienylbenzamide derivative of the present invention has an NPT-IIb inhibitory action and can be used as an agent for preventing and/or treating hyperphosphatemia.
    Type: Grant
    Filed: October 25, 2012
    Date of Patent: June 23, 2015
    Assignee: Astellas Pharma Inc.
    Inventors: Masanori Miura, Daisuke Kaga, Susumu Watanuki, Shunichiro Hachiya, Takao Okuda, Ippei Sato, Mai Isomura, Kazuhiro Terai, Yoh Terada
  • Patent number: 9051307
    Abstract: The present invention relates to novel bipyridyl derivatives of formula (I) and to the use of such compounds in which the inhibition, regulation and/or modulation of signal transduction by ATP consuming proteins like kinases plays a role, particularly to inhibitors of TGF-beta receptor kinases, and to the use of such compounds for the treatment of kinase-induced diseases, in particular for the treatment of tumors.
    Type: Grant
    Filed: July 29, 2014
    Date of Patent: June 9, 2015
    Assignee: Merck Patent GmbH
    Inventors: Guenter Hoelzemann, Dieter Dorsch, Alfred Jonczyk, Christiane Amendt, Frank Zenke
  • Patent number: 9040563
    Abstract: Many GTPases such as Ras, Ral and Rho require post-translational farnestylation or geranylgeranylation for mediating malignant transformation. Dual farnesyltransferase (FT) (FTI) and geranylgeranyltransferase-I (GGT-1) inhibitors (GGTI) were developed as anticancer agents from based on an ethylenediamine scaffold. On the basis of a 4-fold substituted ethylenediamine scaffold, the inhibitors are structurally simple and readily derivatized, facilitating extensive structure-activity relationship studies. The most potent inhibitor is compound exhibited an in vitro hFTase IC50 value of 25 nM and a whole cell H-Ras processing IC50 value of 90 nM. Several of the inhibitors proved highly selective for hFTase over the related prenyltransferase enzyme geranylgeranyltransferase-I (GGTase-I).
    Type: Grant
    Filed: March 11, 2013
    Date of Patent: May 26, 2015
    Assignees: H. Lee Moffitt Cancer Center and Research Institute, Inc., Yale University
    Inventors: Said M. Sebti, Andrew Hamilton
  • Publication number: 20150141463
    Abstract: The present invention provides novel substituted pyrazolone compounds, pharmaceutical acceptable salts and formulations thereof useful in modulating the protein tyrosine kinase activity, and in modulating cellular activities such as proliferation, differentiation, apoptosis, migration and invasion. The invention also provides pharmaceutically acceptable compositions comprising such compounds and methods of using the compositions in the treatment of hyperproliferative disorders in mammals, especially humans.
    Type: Application
    Filed: January 20, 2015
    Publication date: May 21, 2015
    Applicants: CALITOR SCIENCES, LLC, SUNSHINE LAKE PHARMA CO., LTD.
    Inventors: Ning Xi, Yanjun Wu, Min Liao, Yanming Feng
  • Publication number: 20150133473
    Abstract: The present invention provides a compound of formula (A): as described herein, and pharmaceutically acceptable salts, enantiomers, rotamers, tautomers, or racemates thereof. Also provided are methods of treating a disease or condition mediated by PIM kinase using the compounds of Formula I, and pharmaceutical compositions comprising such compounds.
    Type: Application
    Filed: May 20, 2013
    Publication date: May 14, 2015
    Applicant: NOVARTIS AG
    Inventors: Matthew Burger, Joseph E. Drumm III, Gisele Nishiguchi, Alice Rico, Robert Lowell Simmons, Benjamin Taft, Huw Tanner
  • Publication number: 20150133430
    Abstract: Provide herein are compounds and pharmaceutical compositions suitable as modulators of hemoglobin, methods and intermediates for their preparation, and methods for their use in treating disorders mediated by hemoglobin and disorders that would benefit from tissue and/or cellular oxygenation.
    Type: Application
    Filed: January 16, 2015
    Publication date: May 14, 2015
    Inventors: Qing XU, Zhe LI
  • Publication number: 20150126529
    Abstract: Disclosed are azaindazole compounds of Formula (I): or a pharmaceutically acceptable salt thereof, wherein: X is O and Y is N; or X is S and Y is CH; Z is CR2 or N; Q is a heteroaryl; and R1 is defined herein. Also disclosed are methods of using such compounds in the treatment of at least one CYP17 associated condition, such as, for example, cancer, and pharmaceutical compositions comprising such compounds.
    Type: Application
    Filed: January 16, 2015
    Publication date: May 7, 2015
    Inventors: Upender Velaparthi, Peiying Liu
  • Publication number: 20150126496
    Abstract: The invention relates to methods for diagnosis and treatment of autism spectrum disorders, particularly for autism spectrum disorders characterized by increased head size (circumference) and deficits in social behavior.
    Type: Application
    Filed: October 10, 2014
    Publication date: May 7, 2015
    Applicant: Massachusetts Institute of Technology
    Inventors: Damon Theron Page, Mriganka Sur
  • Publication number: 20150126558
    Abstract: To provide crystal polymorphs of 4-[5-(pyridin-4-yl)-1H-1,2,4-triazol-3-yl]pyridine-2-carbonitrile, which is a useful pharmaceutical, and a production method therefor. Through purification of a corresponding salt, recrystallization, or storage under humidified conditions, three different crystal forms; i.e., crystalline polymorphs of 4-[5-(pyridin-4-yl)-1H-1,2,4-triazol-3-yl]pyridine-2-carbonitrile are produced.
    Type: Application
    Filed: July 24, 2013
    Publication date: May 7, 2015
    Applicant: FUJIYAKUHIN CO., LTD.
    Inventors: Yoshiyuki Iwabuchi, Sachiho Miyata, Takahiro Sato, Junichiro Uda, Takamitsu Kandou, Tadashi Inoue, Hiroyuki Nakano