Abstract: The present invention embraces compounds selected for interacting with the Fingers-Palm pocket of telomerase and use thereof for modulating the activity of telomerase and preventing or treating diseases or conditions associated with telomerase.
Abstract: There are disclosed racemic or enantiomerically enriched 3- or 4-substituted piperidine compounds represented by the following structural formula (I): or any of their isomers, or pharmaceutically acceptable salts thereof. Also disclosed are pharmaceutical compositions containing the subject compounds. The subject compounds are useful for the treatment of diseases of the central nervous system, particularly depression, anxiety and pain disorder.
Type:
Grant
Filed:
January 19, 2012
Date of Patent:
August 20, 2013
Assignee:
SK Biopharmaceuticals Co., Ltd.
Inventors:
Ki-Ho Lee, Chun-Eung Park, Kyung-Hyan Min, Yong-Je Shin, Yu-Jin Shin, Hae-Jeong Yoon, Won Kim, Eun-Ju Ryu
Abstract: The present invention provides a method for stabilizing an anti-dementia drug in a pharmaceutical composition containing the anti-dementia drug and a high molecular weight basic substance by adding a high molecular weight acidic substance to said pharmaceutical composition. Further, the present invention provides a pharmaceutical composition containing an anti-dementia drug and a high molecular basic substance in which a high molecular weight acidic substance is contained for stabilizing the anti-dementia drug. Furthermore, the present invention provides a method for manufacturing a pharmaceutical composition which comprises steps wherein a solution or suspension containing a high molecular weight acidic substance is added to a mixture of an anti-dementia drug and a high molecular weight basic substance for the sake of stabilizing the anti-dementia drug.
Abstract: Compounds that selectively modulate the sphingosine 1 phosphate receptor are provided including compounds which modulate subtype 1 of the S1P receptor. Methods of chiral synthesis of such compounds is provided. Uses, methods of treatment or prevention and methods of preparing inventive compositions including inventive compounds are provided in connection with the treatment or prevention of diseases, malconditions, and disorders for which modulation of the sphingosine 1 phosphate receptor is medically indicated.
Type:
Grant
Filed:
November 15, 2010
Date of Patent:
August 13, 2013
Assignee:
Receptos, Inc.
Inventors:
Marcus F. Boehm, Esther Martinborough, Enugurthi Brahmachary, Manisha Moorjani, Junko Tamiya, Liming Huang, Adam Richard Yeager
Abstract: The invention provides compounds of formula (I): or a salt thereof as described herein. The invention also provides pharmaceutical compositions comprising a compound of formula I, processes for preparing compounds of formula (I), intermediates useful for preparing compounds of formula I and therapeutic methods for treating the proliferation of the HIV virus, treating AIDS or delaying the onset of AIDS or ARC symptoms in a mammal using compounds of formula (I).
Type:
Application
Filed:
July 1, 2011
Publication date:
August 8, 2013
Applicant:
GILEAD SCIENCES, INC.
Inventors:
Kerim Babaoglu, Elizabeth Bacon, Kyla Bjornson, Hongyan Guo, Randall L. Halcomb, Paul Hrvatin, John O. Link, Hongtao Liu, Ryan McFadden, Michael L. Mitchell, Paul Roethle, James Taylor, James D. Trenkle, Randall W. Vivian, Lianhong Xu
Abstract: Provided is a patch that ensures high storage stability of donepezil or a salt thereof and allows stable transdermal administration of the donepezil or salt thereof in an amount that provides a pharmaceutical effect. The patch includes a substrate 1 and an adhesive layer 2 stacked on and integrated with one surface of the substrate 1 and containing donepezil or a salt thereof and an acrylic adhesive containing a copolymer obtained by copolymerizing monomers that each contain a (meth)acrylic acid ester of a saturated aliphatic alcohol and do not contain vinylpyrrolidone.
Abstract: This invention comprises the novel compounds of formula (I) wherein t, R1, R2, L, Q, X, Y, Z and have defined meanings, having histone deacetylase inhibiting enzymatic activity; their preparation, compositions containing them and their use as a medicine.
Abstract: The present invention relates to compounds of the Formula (I) that are useful antimicrobial agents and effective against a variety of multi-drug resistant bacteria:
Type:
Grant
Filed:
February 8, 2012
Date of Patent:
August 6, 2013
Assignee:
Morphochem Aktiengesellschaft für Kombinatorische Chemie
Inventors:
Christian Hubschwerlen, Jean-Luc Specklin, Daniel Baeschlin, Christine Schmitt, Stefan Muller, Michael W. Cappi
Abstract: The invention provides aminotetralin compounds of formula (I): wherein R1, R2, R3, R4, R5, R6, R7, n, and m are defined in the specification, or a pharmaceutically-acceptable salt thereof, that are antagonists at the mu opioid receptor. The invention also provides pharmaceutical compositions comprising such compounds, methods of using such compounds to treat conditions associated with mu opioid receptor activity, and processes and intermediates useful for preparing such compounds.
Type:
Grant
Filed:
October 17, 2012
Date of Patent:
July 30, 2013
Assignee:
Theravance, Inc.
Inventors:
Michael R. Leadbetter, Sean G. Trapp, Daniel D. Long, John R. Jacobsen, Sabine Axt
Abstract: The present invention relates to novel 1-(4H-1,3-benzodioxin-2-yl)methanamine derivatives, useful as modulators of dopamine neurotransmission, and more specifically asdopaminergic stabilizers. In other aspects the invention relates to the use of these compounds in a method for therapy and to pharmaceutical compositions comprising the compounds of the invention.
Type:
Grant
Filed:
April 28, 2009
Date of Patent:
July 23, 2013
Assignee:
Integrated Research Laboratories Sweden AB
Inventors:
Clas Sonesson, Peder Svensson, Mikael Andersson
Abstract: Compounds of Formula (I) along with processes for their preparation that are useful for treating, managing and/or lessening the diseases, disorders, syndromes or conditions associated with the modulation of cannabinoid (CB) receptors. Methods of treating, managing and/or lessening the diseases, disorders, syndromes or conditions associated with the modulation of cannabinoid (CB) receptors of Formula (I).
Abstract: The present invention provides a method for stabilizing an anti-dementia drug in a pharmaceutical composition containing the anti-dementia drug and a high molecular weight basic substance by adding a high molecular weight acidic substance to said pharmaceutical composition. Further, the present invention provides a pharmaceutical composition containing an anti-dementia drug and a high molecular basic substance in which a high molecular weight acidic substance is contained for stabilizing the anti-dementia drug. Furthermore, the present invention provides a method for manufacturing a pharmaceutical composition which comprises steps wherein a solution or suspension containing a high molecular weight acidic substance is added to a mixture of an anti-dementia drug and a high molecular weight basic substance for the sake of stabilizing the anti-dementia drug.
Abstract: A method administers quaternary ammonium anti-cholinergic muscarinic receptor antagonists in combination with acetyl-cholinesterase inhibitors to treat either cognitive impairment or acute delirium. This therapy results in a modification of a cognitive disorder or disease, namely a slow down in the disease progression. In one preferred embodiment, the disease is dementia with Lewy Bodies. New formulations for quaternary ammonium anti-cholinergic muscarinic receptor antagonists are also disclosed.
Abstract: The present invention is directed to a compound of the formula (A): or a pharmaceutically acceptable salt thereof; and also to compounds of formula (I): or a pharmaceutically acceptable salt thereof.
Type:
Grant
Filed:
September 3, 2009
Date of Patent:
July 2, 2013
Assignee:
Eli Lilly and Company
Inventors:
Jeffrey Alan Dodge, Timothy Ivo Richardson, Christian Alexander Clarke, Scott Alan Jones, Ronald Jay Hinklin, Conrad Wilson Hummel, George Sal Lewis
Abstract: There is described a method for increasing the maximal tolerated dose and thus the efficacy of an acetyl choline esterase inhibitor (AChEI) in a patient suffering from an Alzheimer type dementia by decreasing concomitant adverse effects by administration of said AChEI in combination with a non-selective, peripheral anticholinergic agent, whereby an enhanced acetyl choline esterase inhibition in the CNS of said patient is achieved and alleviation of the symptoms of Alzheimer type dementia in said patient is thereby improved to a greater extent.
Type:
Application
Filed:
February 12, 2013
Publication date:
June 20, 2013
Applicant:
CHASE PHARMACEUTICALS CORPORATION
Inventors:
Thomas N. Chase, Kathleen E. Clarence-Smith
Abstract: The invention is concerned with the compounds of formula (I): and pharmaceutically acceptable salts thereof, wherein R1, R2, R3 and X are defined in the detailed description and claims. In addition, the present invention relates to methods of manufacturing and using the compounds of formula I as well as pharmaceutical compositions containing such compounds. The compounds of formula I are antagonists or partial agonists at the CRTH2 receptor and may be useful in treating diseases and disorders associated with that receptor such as asthma.
Abstract: The present invention provides compounds, or derivatives or prodrugs thereof, that comprise a methyllysine mimic, and an ?-ketoglutarate mimic that are attached through a linker and methods for using and producing the same. In some embodiments, compounds of the invention are of the formula: M-L-K, or a derivative or a prodrug thereof, wherein M is a methyllysine mimic, L is a linker, and K is an ?-ketoglutarate mimic.
Type:
Application
Filed:
November 30, 2012
Publication date:
May 30, 2013
Applicant:
The Regents of the University of Colorado, a body corporated
Abstract: The present invention relates to compounds of formula (I), where R1 and R2, which may be identical or different, are selected from the group comprising H, CnH2n-1, a linear or branched alkyl group having 1 to 6 carbons, or together form an aromatic or aliphatic ring with 5 or 6 atoms; R3 is —CO—CH3, —NHOH, —OH, or —OR6 where R6 is a linear or branched alkyl group having 1 to 6 carbon atoms; R4 is H, linear or branched alkyl group having from 1 to 6 atoms, phenyl, benzyl, —CF3 or CF2CF3, vinyl or allyl; R5, R7, R8 are hydrogen atoms; or R3 and R4, R4 and R5, or R7 and R8 together form a ring, fused to the benzene, aromatic or aliphatic ring with 5 or 6 atoms comprising from 1 to 2 heteroatoms selected independently from the group comprising N, O, and use thereof in the medical field.
Abstract: Described herein are methods for modulation of the activity of the carotid body that afford therapeutic benefit for sleep-related breathing disorders and related conditions.
Type:
Application
Filed:
April 11, 2011
Publication date:
May 23, 2013
Applicants:
JOHNS HOPKINS UNIVERSITY, SOVA PHARMACEUTICALS, INC., THE UNIVERSITY OF CHICAGO
Inventors:
Solomon H. Snyder, Moataz M. Gadalla, Nanduri R. Prabhakar, Gregory Stein, Gary Pace
Abstract: The instant invention relates to derivatives of formula (I) and their application in therapeutics.
Type:
Application
Filed:
March 1, 2011
Publication date:
May 23, 2013
Applicant:
SANOFI
Inventors:
Markus Follmann, Pascale Goberville, Stéphanie Hachtel, Gerhard Hessler, Heinz-Werner Kleemann, Thomas Maier, Gary MC Cort, Carsten Struebing, Bérangère Thiers, Li-Hsing Wang
Abstract: The present invention is directed to a compound of formula (I) for use in a method to treat or ameliorate amyloid or tau pathologies, such as Alzheimer's disease, or symptoms thereof. The invention is also directed to new compounds of formula (I), of subformula (II), (III), (IV), or (V).
Type:
Application
Filed:
May 23, 2011
Publication date:
May 23, 2013
Applicant:
FAES FARMA, S.A.
Inventors:
Francisco Ledo Gómez, Ana Muñoz Muñoz, Carmen Pumar Durán
Abstract: This invention provides, but is not limited to, novel oleanolic acid derivatives having the formula: wherein the variables are defined herein. Also provided are pharmaceutical compositions, kits and articles of manufacture comprising such compounds, methods and intermediates useful for making the compounds, and methods of using the compounds and compositions.
Type:
Grant
Filed:
January 23, 2012
Date of Patent:
May 14, 2013
Assignee:
Reata Pharmaceuticals, Inc.
Inventors:
Eric Anderson, Xin Jiang, Melean Visnick
Abstract: Compounds of the formula (I), in which R1, R2, R3, R4, R5, R6, R9, R10, R11, Q and W have the meanings indicated in Claim 1, and precursors thereof are inhibitors of sphingosine kinase and can be employed, inter alia, for the treatment of tumors.
Type:
Grant
Filed:
May 28, 2009
Date of Patent:
May 7, 2013
Assignee:
Merck Patent Gesellschaft mit beschrankter Haftung
Inventors:
Frank Stieber, Timo Heinrich, Dirk Wienke
Abstract: The present invention relates to combinations and methods for the treatment of neurological disorders related to glutamate excitotoxicity and Amyloid ? toxicity. More specifically, the present invention relates to novel combinatorial therapies of Multiple Sclerosis, Alzheimer's disease, Alzheimer's disease related disorder, Amyotrophic Lateral Sclerosis, Parkinson's disease, Huntington's disease, neuropathic pain, alcoholic neuropathy, alcoholism or alcohol withdrawal, or spinal cord injury, based on Baclofen and Acamprosate combination.
Abstract: The present application describes deuterium-enriched donepezil, pharmaceutically acceptable salt forms thereof, and methods of treating using the same.
Abstract: The present invention relates to combinations and methods for the treatment of neurological disorders related to glutamate excitotoxicity and Amyloid ? toxicity. More specifically, the present invention relates to novel combinatorial therapies of Multiple Sclerosis, Alzheimer's disease, Alzheimer's disease related disorder, Amyotrophic Lateral Sclerosis, Parkinson's disease, Huntington's disease, neuropathic pain, alcoholic neuropathy, alcoholism or alcohol withdrawal, or spinal cord injury, based on Baclofen and Acamprosate combination.
Abstract: Methods of treating, preventing and/or managing myelodysplastic syndromes are disclosed. Specific methods encompass the administrations of 3-(4-amino-1-oxo-1,3-dihydro-isoindol-2-yl)-piperidin-2,6-dione in combination with 5-azacytidine.
Abstract: Methods of treating, preventing and/or managing myelodysplastic syndromes are disclosed. Specific methods encompass the administrations of 3-(4-amino-1-oxo-1,3-dihydro-isoindol-2-yl)-piperidin-2,6-dione in combination with 5-azacytidine.
Abstract: Inhibitors of retroviral propagation, methods of treatment and prevention of retroviral infections using the inhibitors, and pharmaceutical compositions including the inhibitors, are disclosed.
Abstract: Compounds of formula (I) as well as pharmaceutically acceptable salts thereof can be used in the form of pharmaceutical compositions, wherein A1, A2, R1, R2, R3 and R4 have the significance given in claim 1.
Type:
Grant
Filed:
July 23, 2010
Date of Patent:
March 19, 2013
Assignee:
Hoffman-La Roche Inc.
Inventors:
Jean Ackermann, Aurelia Conte, Daniel Hunziker, Werner Neidhart, Matthias Nettekoven, Stanley Wertheimer
Abstract: A method of making a pharmaceutical tablet comprises (a) combining (i) an aqueous networked cellulose gel with (ii) filler and (iii) an active agent to form a mixture thereof; (b) casting the mixture to form a wet tablet; (c) drying the wet tablet to form a dry pharmaceutical tablet; and then (d) optionally coating the tablet (e.g., with an enteric coating). Pharmaceutical tablets produced by such methods are also described.
Abstract: This invention comprises the novel compounds of formula (I) wherein n, m, t, R1, R2, R3, R4, R5, L, Q, X, Y and have defined meanings, having histone deacetylase inhibiting enzymatic activity; their preparation, compositions containing them and their use as a medicine.
Type:
Grant
Filed:
October 24, 2011
Date of Patent:
March 12, 2013
Assignee:
Janssen Pharmaceutica, N.V.
Inventors:
Kristof Van Emelen, Marc Gustaaf Celine Verdonck, Sven Franciscus Anna Van Brandt, Leo Jacobus Jozef Backx
Abstract: A medicament for prophylactic and/or therapeutic treatment of Alzheimer-type dementia, which comprises donepezil hydrochloride and valproic acid or a salt thereof in combination.
Type:
Application
Filed:
November 7, 2012
Publication date:
March 7, 2013
Applicants:
KOWA COMPANY, LTD., NAGOYA CITY UNIVERSITY
Inventors:
Nagoya City University, Kowa Company, Ltd.
Abstract: Sustained release formulations comprising donepezil, or its pharmaceutically acceptable salts, and methods of preparing the sustained release formulations.
Type:
Application
Filed:
December 3, 2010
Publication date:
March 7, 2013
Applicants:
DR. REDDY'S LABORATORIES, INC., DR. REDDY'S LABORATORIES LTD.
Abstract: Novel methods for the medical treatment and/or inhibition of the development of osteoporosis, breast cancer, hypercholesterolemia, hyperlipidemia or atherosclerosis in susceptible warm-blooded animals including humans involving administration of selective estrogen receptor modulator particularly compounds having the general structure: and an amount of a sex steroid precursor selected from the group consisting of dehydroepiandrosterone, dehydroepiandrosterone sulfate, androst-5-ene-3?,17?-diol and compounds converted in vivo to one of the foregoing presursor. Further administration of bisphosphonates in combination with selective estrogen receptor modulators and/or sex steroid precursor is disclosed for the medical treatment and/or inhibition of the development of osteoporosis. Pharmaceutical compositions for delivery of active ingredient(s) and kit(s) useful to the invention are also disclosed.
Abstract: Provided is a transdermal preparation having low skin irritation as well as a sufficient skin permeability rate of donepezil, which comprises one or more drugs selected from donepezil and pharmaceutically acceptable salts thereof. Also provided are a manufacturing method thereof, and a method for reducing skin irritation of a transdermally absorbable donepezil-containing preparation. An embodiment is a transdermal preparation comprising one or more drugs selected from donepezil and pharmaceutically acceptable salts thereof, and a skin irritation-reducing agent.
Abstract: The invention provides aminotetralin compounds of formula (I): wherein R1, R2, R3, R4, R5, R6, R7, n, and m are defined in the specification, or a pharmaceutically-acceptable salt thereof, that are antagonists at the mu opioid receptor. The invention also provides pharmaceutical compositions comprising such compounds, methods of using such compounds to treat conditions associated with mu opioid receptor activity, and processes and intermediates useful for preparing such compounds.
Type:
Application
Filed:
October 17, 2012
Publication date:
February 14, 2013
Applicant:
THERAVANCE, INC.
Inventors:
Michael R. Leadbetter, Sean G. Trapp, Daniel D. Long, John R. Jacobsen, Sabine Axt
Abstract: Disclosed herein is a pharmaceutical composition comprising a cholinesterase inhibitor and compound of the following formula: The composition is effective for treating cognitive disorders, and methods of treating such disorders using the composition are also disclosed.
Abstract: A pharmaceutical formulation of compounds with low aqueous solubility and method of manufacture thereof. The formulation may include a pharmacologically active compound having low aqueous solubility and starch in the amount of greater than about 25 weight percent. A manufacturing method may include blending the active compound and starch, compressing the blend into a solid, comminuting the solid into granules, wetting the granules, drying the granules, and tabletting the dried granules to make a solid pharmaceutical formulation.
Type:
Grant
Filed:
November 10, 2004
Date of Patent:
February 5, 2013
Assignee:
Teva Pharmaceutical Industries, Ltd.
Inventors:
Ilan Zalit, Fanny Leska, Mali Kadosh, Dorit Marco, Yonit Messer-Triger
Abstract: A medicament delivery system is disclosed. The system comprises a descending formulation for delivering the medicament and an ascending formulation to protect a patient being treated with the medicament from the side effects thereof.
Abstract: The present invention relates to a pharmaceutical composition of donepezil or pharmaceutically acceptable salts thereof comprising ethyl cellulose and methacrylic acid copolymer in a ratio of more than 1.3. Further, it relates to process for preparation of said composition.
Abstract: The present invention relates to a percutaneous absorption preparation which can administer an anti-dementia drug stably and efficiently for a long period such as one week. More specifically, the present invention relates to a percutaneous absorption preparation comprising a drug-containing layer comprising an anti-dementia drug, a polymer compound having an amino group, a polyhydric alcohol fatty acid ester, a polyhydric alcohol, a polyvalent carboxylate ester, and a styrenic polymer compound.
Abstract: Pulmonary arterial hypertension in a mammal can be prevented or treated using combined 5-HT2A and 5-HT2B receptor antagonist. The antagonists can be present in a single compound or in two separate compounds.
Abstract: Certain compounds and pharmaceutically acceptable salts are provided herein. Also provided are pharmaceutical compositions comprising at least one compound or pharmaceutically acceptable salt therein and one or more pharmaceutically acceptable vehicle. Methods of treating patients suffering from certain disease states responsive to the inhibition of transglutaminase TG2 activity are described. These disease states include neurodegenerative disorders such as Huntington's disease. Also described are methods of treatment include administering at least one compound or pharmaceutically acceptable salt thereof as a single active agent or administering at least one compound or pharmaceutically acceptable salt thereof in combination with one or more other therapeutic agents.
Type:
Application
Filed:
May 7, 2012
Publication date:
November 29, 2012
Inventors:
Michael Prime, Stephen Martin Courtney, Richard Marston, Celia Dominguez, Douglas Macdonald, John Wityak
Abstract: There are provided compounds and methods for the detection and treatment of amyloid deposits and diseases and disorders characterized by amyloid deposits including Alzheimer's disease and related amyloid-based neurodegenerative disorders.
Type:
Application
Filed:
December 10, 2010
Publication date:
November 29, 2012
Applicant:
THE REGENTS OF THE UNIVERSITY OF CALIFORNIA
Abstract: Provided is an oral preparation that contains a medicinal component having an unpleasant taste and that has better qualities, for example, generation of an analogue can be reduced, better than oral preparations that are produced by conventional techniques and that contain a medicinal component having an unpleasant taste. This objective is achieved by adding a coating agent on the medicinal component and a disintegrator that has a carboxymethyl group.
Type:
Application
Filed:
December 28, 2010
Publication date:
November 22, 2012
Applicant:
NIPRO CORPORATION
Inventors:
Kennichiro Kuninobu, Yohei Hoashi, Naohisa Katayama, Toshiya Kai
Abstract: The invention relates to compounds corresponding to the general formula (I): in which R2 represents a hydrogen, fluorine, hydroxyl, cyano, trifluoromethyl, C1-6-alkyl, C1-6-alkoxy or —NR8R9; n and m represent, independently of one another, an integer equal to 1, 2 or 3, it being understood that the sum m+n is at most equal to 5; A represents a covalent bond, an oxygen, a C1-6-alkylene or —O—C1-6-alkylene; R1 represents a phenyl or a heterocycle which is optionally substituted; R3 represents a hydrogen, fluorine, C1-6-alkyl or trifluoromethyl; R4 represents an optionally substituted 5-membered heterocycle; in the form of the base or of an addition salt with an acid; with the exclusion of 5-methylisoxazol-3-ylmethyl 4-hydroxy-4-(4-chlorophenyl)piperidine-1-carboxylate. The invention also relates to a process for the preparation of the compounds of formula (I), to compositions comprising them and to their therapeutic application.
Abstract: The invention provides aminotetralin compounds of formula (I): wherein R1, R2, R3, R4, R5, R6, R7, n, and m are defined in the specification, or a pharmaceutically-acceptable salt thereof, that are antagonists at the mu opioid receptor. The invention also provides pharmaceutical compositions comprising such compounds, methods of using such compounds to treat conditions associated with mu opioid receptor activity, and processes and intermediates useful for preparing such compounds.
Type:
Grant
Filed:
December 19, 2011
Date of Patent:
November 20, 2012
Assignee:
Theravance, Inc.
Inventors:
Michael R. Leadbetter, Sean G. Trapp, Daniel D. Long, John R. Jacobsen, Sabine Axt