Abstract: The present invention is related to a method of determining a test compound's ability to modify the biological activity of a GPR17. Said method comprises, among others, the step of contacting the test compound with a GPR17, or a functional GPR17 fragment in the presence of a suitable amount of a GPR17 agonist of formula I.
Abstract: The invention provides novel compounds having the general formula: wherein X1 is N or N+O?, and one of X2, X3 and X4 is N or N+—O? and the remainder of X2, X3 and X4 is C. R2, R3, R4, R5, R6. A, B and Y are as described herein. Additionally compositions compounds of Formula I and methods of use are further described herein.
Type:
Grant
Filed:
December 14, 2011
Date of Patent:
January 7, 2014
Assignee:
Genentech, Inc.
Inventors:
Joseph P. Lyssikatos, Lewis J. Gazzard, Emily Hanan, Samuel Kintz, Hans Edward Purkey
Abstract: This disclosure concerns novel compounds of Formula (I) or as defined in the specification and compositions comprising such novel compounds. These compounds are useful antiviral agents, especially in inhibiting the function of the NS5A protein encoded by Hepatitis C virus (HCV). Thus, the disclosure also concerns a method of treating HCV related diseases or conditions by use of these novel compounds or a composition comprising such novel compounds.
Abstract: The present invention relates to methods and compounds for regulating or enhancing erythropoiesis and iron metabolism, and for treating or preventing iron deficiency and anemia of chronic disease.
Type:
Grant
Filed:
June 3, 2004
Date of Patent:
December 24, 2013
Assignee:
Fibrogen, Inc.
Inventors:
Stephen J. Klaus, Christopher J. Molineaux, Thomas B. Neff, Volkmar Guenzler-Pukall, Ingrid Langsetmo Parobok, Todd W. Seeley, Robert C. Stephenson
Abstract: The present invention relates to methods and compounds for decreasing the expression of hepcidin, a protein associated with regulation of iron metabolism.
Type:
Grant
Filed:
July 12, 2010
Date of Patent:
December 17, 2013
Assignee:
Fibrogen, Inc.
Inventors:
Stephen J. Klaus, Christopher J. Molineaux, Thomas B. Neff, Volkmar Guenzler-Pukall, Ingrid Langsetmo Parobok, Todd W. Seeley, Robert C. Stephenson
Abstract: The present invention relates to compositions, kits and methods for treating skin at sites of concerns such as infectious lesions and/or points of insertion of an insertable medical device to prevent contamination such as infections or protein absorption that may interfere with the function of the device. The composition can be a topical skin treatment composition that includes polyethylene glycol (PEG), triclosan, one or more of a salicylate, bronopol, and an acrylic emulsion, and, optionally, a solvent.
Abstract: The present invention relates to methods for treating anemia in a subject having a low percent transferrin saturation by administering to the subject an effective amount of a compound that inhibits hypoxia-inducible factor prolyl hydroxylase activity.
Type:
Grant
Filed:
July 12, 2010
Date of Patent:
December 10, 2013
Assignee:
Fibrogen, Inc.
Inventors:
Stephen J. Klaus, Christopher J. Molineaux, Thomas B. Neff, Volkmar Guenzler-Pukall, Ingrid Langsetmo Parobok, Todd W. Seeley, Robert C. Stephenson
Abstract: The present invention relates to methods and compounds for increasing serum iron in a subject.
Type:
Grant
Filed:
July 12, 2010
Date of Patent:
December 10, 2013
Assignee:
Fibrogen, Inc.
Inventors:
Stephen J. Klaus, Christopher J. Molineaux, Thomas B. Neff, Volkmar Guenzler-Pukall, Ingrid Langsetmo Parobok, Todd W. Seeley, Robert C. Stephenson
Abstract: The present invention provides a low molecular weight compound having EPO production-promoting action and/or hemoglobin production-promoting action. The present invention relates to a fused piperidine compound represented by the following general formula (1): (wherein, ring A represents a C10-14 aryl group or 5- to 10-membered heterocyclic group, X represents N—R7, a sulfur atom or an oxygen atom, R1, R2, R2?, R3 and R3? independently represent a hydrogen atom, C1-6 alkyl group or C3-6 cycloalkyl group, and R4, R5 and R6 independently represent a hydrogen atom or halogen atom), or a salt thereof, or a solvate thereof.
Abstract: The invention relates to compounds for inhibiting the Cyclin-Dependent Kinase Inhibitor (CDKI) pathway. More particularly, the invention relates to compounds for inhibiting the CDKI pathway for studies of and intervention in senescence-related and other CDKI-related diseases.
Type:
Grant
Filed:
November 30, 2010
Date of Patent:
December 3, 2013
Assignee:
Senex Biotechnology
Inventors:
Donald C. Porter, Igor B. Roninson, Mark P. Wentland
Abstract: Disclosed are compounds of Formula (I) and methods of using compounds of the invention for treating a subject with a proliferative disorder, such as cancer, and methods for treating disorders responsive to Hsp70 induction and/or natural killer induction. Also, disclosed are pharmaceutical compositions comprising compounds of the invention and a pharmaceutically acceptable carrier.
Abstract: A compound with general formula I for treatment of various diseases of the central nervous system, in treatment of neuropsychiatric disorders related to imbalance of glutamatergic neurotransmitter system, ischemic damage of CNS, neurodegenerative changes and disorders of CNS, affective disorders, depression, PTSD and other diseases related to stress, anxiety, schizophrenia and psychotic disorders, pain, addictions, multiple sclerosis, epilepsy and gliomas.
Type:
Grant
Filed:
May 28, 2010
Date of Patent:
November 5, 2013
Assignees:
Ustav Organicke Chemie A Biochemie Akademie Ved Ceske Republiky, V.V.I., Fyziologicky Ustav Akadamie Ved Ceske Republiky, V.V.I., Psychiatricke Centrum Praha
Inventors:
Hana Chodounska, Eva Stastna, Vojtech Kapras, Ladislav Kohout, Jirina Borovska, Ladislav Vyklicky, Karel Vales, Ondrej Cais, Lukas Rambousek, Ales Stuchlik, Vera Valesova
Abstract: The present invention relates to formulations of (R)-1-(2,2-difluorobenzo[d][1,3]dioxol-5-yl)-N-(1-(2,3-dihydroxypropyl)-6-fluoro-2-(1-hydroxy-2-methylpropan-2-yl)-1H-indol-5-yl)cyclopropanecarboxamide (Compound 1), pharmaceutical packs or kits thereof, and methods of treatment therewith.
Type:
Grant
Filed:
June 8, 2011
Date of Patent:
October 22, 2013
Assignee:
Vertex Pharmaceuticals Incorporated
Inventors:
Rossitza Gueorguieva Alargova, Irina Nikolaevna Kadiyala, Noreen Tasneem Zaman
Abstract: Described herein are ways to solubilize clopidogrel for parenteral administration containing clopidogrel and a diluent NNDMA (N,N-dimethylacetamide); useful in the prevention of platelet aggregation in acute coronary syndrome, acute myocardial infarction or to prevent platelet facilitated thrombosis following coronary angioplasty and/or coronary stenting.
Abstract: Disclosed are compounds of the formula (I), useful for treating a variety of diseases and disorders that are mediated or sustained through the activity of CCR1 including autoimmune diseases, such as rheumatoid arthritis and multiple sclerosis. Also disclosed are methods of making and methods of using same.
Type:
Grant
Filed:
December 16, 2011
Date of Patent:
October 1, 2013
Assignee:
Boehringer Ingelheim International GmbH
Inventors:
Rajashekhar Betageri, Brian Nicholas Cook, Darren DiSalvo, Christian Harcken, Daniel Kuzmich, Pingrong Liu, John Lord, Can Mao, Hossein Razavi
Abstract: The invention provides use of a photosensitiser, which is a derivative (e.g., an ester) of 5-aminolevulinic acid (5-ALA) or a pharmaceutically acceptable salt thereof, in the manufacture of a medicament for use in the prevention or treatment of acne.
Type:
Grant
Filed:
November 9, 2012
Date of Patent:
October 1, 2013
Assignee:
Photocure ASA
Inventors:
Aslak Godal, Jo Klaveness, Hilde Morris
Abstract: The present invention encompasses compounds of general formula (I) wherein the groups R5 to R10, A, L1, B, m and p are defined as in claim 1, which are suitable for the treatment of diseases characterized by excessive or abnormal cell proliferation, pharmaceutical preparations which contain such compounds and their use as medicaments.
Type:
Grant
Filed:
December 19, 2011
Date of Patent:
October 1, 2013
Assignee:
Boehringer Ingelheim International GmbH
Inventors:
Matthias Treu, Stephan Karl Zahn, Patricia Amouzegh, Cristina Lecci, Heather Tye
Abstract: The present invention relates to phosphonated Rifamycins, and methods of making and using such compounds. These compounds are useful as antibiotics for prophylaxis and/or the treatment of bone and joint infections, especially for the prophylaxis and/or treatment of osteomyelitis.
Type:
Grant
Filed:
August 10, 2009
Date of Patent:
September 3, 2013
Assignee:
The Medicines Company
Inventors:
Evelyne Dietrich, Ranga Reddy, Kelly Tanaka, Ting Kang, Yanick LaFontaine, Adel Rafai Far
Abstract: The disclosure provides compounds of formula I, including their salts, as well as compositions and methods of using the compounds. The compounds have activity against hepatitis C virus (HCV) and may be useful in treating those infected with HCV.
Type:
Grant
Filed:
December 5, 2011
Date of Patent:
August 13, 2013
Assignee:
Bristol-Myers Squibb Company
Inventors:
Kap-Sun Yeung, John F. Kadow, Rajesh Onkardas Bora, Kumaravel Selvakumar
Abstract: The invention provides to a family of aryl guanidine—based F1F0—ATPase inhibitors, e.g., mitochondrial F1F0—ATPase inhibitors, methods for their discovery, and their use as therapeutic agents for treating certain disorders.
Type:
Grant
Filed:
September 11, 2009
Date of Patent:
July 30, 2013
Assignee:
The Regents of the University of Michigan