Ether Oxygen Single Bonded To Carboxylic Acid, Percarboxylic Acid Or Salt Thereof Through An Acyclic Carbon Or Acyclic Carbon Chain Patents (Class 514/571)
Abstract: Novel compounds of the general formula (I), the use of these compounds as pharmaceutical compositions, pharmaceutical compositions comprising the compounds and methods of treatment employing these compounds and compositions. The present compounds may be useful in the treatment and/or prevention of conditions mediated by Peroxisome proliferator-activated receptors (PPAR), in particular the PPAR? suptype.
Type:
Application
Filed:
April 30, 2010
Publication date:
August 19, 2010
Applicant:
HIGH POINT PHARMACEUTICALS, LLC
Inventors:
Miroslav Havranek, Per Sauerberg, Ingrid Pettersson
Abstract: Amorphous HMG CoA reductase inhibitors, especially amorphous atorvastatin, are described. Also described are pharmaceutical combinations comprising amorphous HMG CoA reductase inhibitors in combination with cholesterol absorption inhibitors or fibrates. A method of manufacturing the compositions using a hot melt extrusion process are also described.
Abstract: The invention provides novel omega-3 oil formulations comprising fenofibrate and a statin. These formulations are effective in small volumes. Related methods of treatment are also described.
Type:
Grant
Filed:
August 3, 2006
Date of Patent:
August 10, 2010
Assignee:
TransForm Pharmaceuticals, Inc.
Inventors:
Orn Almarsson, Hector Guzman, Carolyn Jordan, Julius Remenar
Abstract: There is provided combination products comprising (a) a mast cell inhibitor, or a pharmaceutically-acceptable salt or solvate thereof; and (b) a PPARY agonist, or a pharmaceutically-acceptable salt or solvate thereof. Such combination products find particular utility in atherosclerosis and related conditions.
Abstract: The present invention provides compositions and methods for treating glaucoma, ocular hypertension, and age-related macular degeneration. More specifically, the present invention describes the use of agents that down-regulate expression of tanis and/or p21Waf1/Cip1/Sd1 genes to treat such disorders of the eye.
Type:
Application
Filed:
March 8, 2010
Publication date:
July 8, 2010
Applicant:
ALCON, INC.
Inventors:
Colene D. Drace, Gary W. Williams, Curtis R. Kelly, Najam A. Sharif
Abstract: The invention relates to substituted phenoxyacetic acids of formula (I), where the variables are as defined in claim 1, as useful pharmaceutical compounds for treating respiratory disorders, pharmaceutical compositions containing them, and processes for their preparation.
Type:
Grant
Filed:
August 22, 2005
Date of Patent:
June 15, 2010
Assignee:
AstraZeneca AB
Inventors:
Timothy Jon Luker, Timothy Nicholas Birkinshaw, Rukhsana Tasneem Mohammed
Abstract: The invention relates to compounds of the formula I: and to the pharmaceutically acceptable salts thereof, to processes for the preparation of them and to pharmaceutical compositions comprising them, which are useful especially for the treatment and prevention of dyslipidaemia, atherosclerosis and diabetes.
Type:
Grant
Filed:
August 11, 2003
Date of Patent:
June 15, 2010
Assignee:
Merck Patent GmbH
Inventors:
Michel Brunet, Jean-Jacques Zeiller, Gérard Ferrand, Yves Bonhomme
Abstract: A pharmaceutical composition comprising a compound of formula (1) in polymorphic crystalline Form A: together with a pharmaceutically acceptable carrier or excipient, wherein the compound of formula (1) is present in polymorphic Form A (see, e.g., FIG. 6) substantially free of other polymorphic forms.
Type:
Grant
Filed:
April 21, 2008
Date of Patent:
June 1, 2010
Assignee:
Medicinova, Inc.
Inventors:
Kenneth Walter Locke, David Gregory Roe
Abstract: The invention concerns compositions comprising substituted 1,3-diphenylprop-2-en-1-one derivatives designed for therapeutic use. The inventive compositions are useful in particular for preventing or treating cardiovascular diseases, syndrome X, Ia restenosis, diabetes, obesity, hypertension, inflammatory diseases, cancers or neoplasms (benign or malignant tumors), neurodegenerative, dermatological diseases and disorders related to oxidative stress, for preventing or treating the effects of ageing in general and for example skin ageing, in particular in the field of cosmetics (occurrence of wrinkles and the like).
Abstract: Methods are provided for treating a subject for a condition. In accordance with the subject methods, at least a portion of a subject's autonomic nervous system is modulated during at least one predetermined phase of the subject's menstrual cycle to alter the parasympathetic activity/sympathetic activity ratio in a manner that is effective to treat the subject for the condition. The subject methods find use in the treatment of a variety of different conditions, including various disease conditions, that increase in severity and/or occurrence during one or more phases of the menstrual cycle. Also provided are systems and kits for use in practicing the subject methods.
Type:
Application
Filed:
December 24, 2009
Publication date:
May 13, 2010
Inventors:
Anthony Joonkyoo Yun, Partic Yuarn-Bor Lee
Abstract: A formulation comprising i) fenofibric acid, a physiologically acceptable salt or derivative thereof a other active substances, ii) a binder component comprising at least one enteric binder, and optionally iii) other physiologically ceptable excipients is described. Fenofibric acid, the physiologically acceptable salt or derivative thereof is preferably in the form of a molecular dispersion in these formulations. An advantageous process for their preparation, in particular by melt extrusion, and the use of this formulation for oral administration of fenofibric acid, a physiologically acceptable salt or derivative thereof are likewise described.
Type:
Application
Filed:
August 30, 2009
Publication date:
April 1, 2010
Inventors:
Joerg Rosenberg, Matthias Degenhardt, Joerg Breitenbach, Tom L. Reiland, Kennan C. Marsh
Abstract: This invention relates to methods for treating, preventing, or reversing brain disease or damage produced by chronic alcohol intake by administering a peroxisome proliferator activated receptor (PPAR) agonist.
Type:
Application
Filed:
September 10, 2007
Publication date:
March 4, 2010
Inventors:
Jack Raymond Wands, Suzanne Marie de la Monte
Abstract: This invention relates to methods for treating, preventing, or reversing liver disease or damage produced by chronic alcohol intake by administering at least one peroxisome proliferator activated receptor (PPAR) agonist.
Type:
Application
Filed:
September 10, 2007
Publication date:
January 28, 2010
Inventors:
Suzanne Marie de la Monte, Jack Raymond Wands
Abstract: Disclosed herein are novel compounds, their use in the treatment and prevention of joint and/or cartilage inflammation that provide an alternative to the NSAIDS and selective COX-2 inhibitors by activating endogenous detoxifying cellular defense mechanisms that act to neutralize toxic cellular intermediate. These compounds are PPAR-alpha agonists and/or phase 2 gene activators.
Type:
Application
Filed:
April 30, 2007
Publication date:
January 21, 2010
Inventors:
Konstantinos Konstantopoulos, Paul Talalay, Zachary R. Healy
Abstract: The invention provides novel omega-3 oil solutions of one or more statins. These solutions are readily bioavailable. Notably, because the solutions of the invention contain an omega-3 oil as the major ingredient, they not only provide an antihypercholesterolemic effect due to the statin active ingredient, they also provide recommended daily dosages of omega-3 oils (i.e., approximately 1 gram of omega-3 oil per day), or a portion thereof. The invention also provides novel salts of one or more statins.
Type:
Grant
Filed:
August 5, 2005
Date of Patent:
January 5, 2010
Assignee:
Transform Pharmaceuticals, Inc.
Inventors:
Hector Guzman, Julius Remenar, Orn Almarsson
Abstract: The invention features 4-((phenoxyalkyl)thio)-phenoxyacetic acids and analogs, compositions containing them, and methods of using them as PPAR delta modulators to treat or inhibit the progression of, for example, dyslipidemia.
Type:
Grant
Filed:
October 15, 2007
Date of Patent:
December 22, 2009
Assignee:
Janssen Pharmaceutica NV
Inventors:
Gee-Hong Kuo, Rui Zhang, Aihua Wang, Alan R. DeAngelis
Abstract: The present, invention provides an oral delivery system for a therapeutic compound that is an acid, a salt of an acid or an unionized compound or a proactive form thereof with pharmacological, physiological or biochemical activity. The present invention particularly provides a swallow formulation comprising a therapeutic compound that is an acid, a salt of an acid or an unionized compound or a proactive form thereof which facilitates the rapid delivery of the therapeutic compound to the circulatory system.
Type:
Application
Filed:
November 28, 2006
Publication date:
December 17, 2009
Applicant:
IMAGINOT PTY LTD
Inventors:
Michael Stephen Roberts, George Alexander Davidson, Ruoying Jiang, Geraldine Ann Elliott, Keivan Bezanehtak, Stephen Douglas Chandler, Greg Davey, Mantu Sarkar
Abstract: Compounds of the formula (I): in which R, R1, R2 and R3 are as defined in the description, the use thereof for the treatment of dyslipidaemia, atherosclerosis and diabetes, pharmaceutical compositions comprising them, and processes for the preparation of these compounds.
Type:
Grant
Filed:
April 6, 2005
Date of Patent:
December 15, 2009
Assignee:
Merck Patent Gesellschaft mit beschrankter
Inventors:
Jean Jacques Zeiller, Hervè Dumas, Valérie Guyard-Dangremont, Isabelle Berard, Francis Contard, Daniel Guerrier, Gèrard Ferrand, Yves Bonhomme
Abstract: A method for treating irritable bowel syndrome (IBS) is included. The method includes the step of administering a fibric acid derivative to a patient diagnosed with IBS in order to alleviate the symptoms associated with IBS.
Abstract: The invention features 4-((phenoxyalkyl)thio)-phenoxyacetic acids and analogs, compositions containing them, and methods of using them as PPAR delta modulators to treat or inhibit the progression of, for example, dyslipidemia.
Type:
Grant
Filed:
September 16, 2004
Date of Patent:
October 6, 2009
Assignee:
Janssen Pharmaceutica, N.V.
Inventors:
Gee-Hong Kuo, Rui Zhang, Aihua Wang, Alan R. DeAngelis
Abstract: The present invention is directed toward the use of thyromimetic compounds that are thyroid receptor ligands, pharmaceutically acceptable salts thereof, and to prodrugs of these compounds for preventing, treating, or ameliorating fatty liver diseases such as steatosis, non-alcoholic fatty liver disease, and non-alcoholic steatohepatitis.
Abstract: Provided herein are compounds of the formula (I): as well as pharmaceutically acceptable salts thereof, wherein the substituents are as those disclosed in the specification.
Type:
Application
Filed:
February 23, 2009
Publication date:
September 10, 2009
Inventors:
Romyr Dominique, Robert Alan Goodnow, JR., Agnieszka Kowalczyk, Jianping Lou, Qi Qiao, Achyutharao Siddurl, Jefferson Wright Tilley
Abstract: Methods of modifying taste sensation in an animal are provided. These methods comprise administrating compounds that modulate T1R1/T1R3 or T1R2/T1R3 receptors.
Type:
Application
Filed:
November 13, 2008
Publication date:
September 3, 2009
Applicant:
Senomyx, Inc.
Inventors:
Mark Zoller, Xiaodong Li, Lena Staszewski, Shawn O'Connell, Sergey Zozulya, Jon Elliot Adler, Hong Xu, Fernando Echeverri
Abstract: Medicine, in particular broad spectrum medicinal preparations. This invention is based on the use of 4-chlorine-2-methyl-phenoxy-acetic acid of formula I, the pharmacologically acceptable derivatives thereof, for example on corresponding alkali metal salts of the acid and the derivatives in the form of pharmaceutical preparations exhibiting immunomodulating, anti-inflammatory and anti-tumoral properties and antiviral activity. The broad spectrum of therapeutic modalities of the inventive medicinal preparation and the fact that it does not produce side effects are proven by study.
Abstract: The invention relates generally to the field of treatment of headache, post-laminectomy syndrome, and other disorders associated with localized pain. The compositions and methods described herein are useful for alleviating both the disorders and the pain associated therewith.
Abstract: Novel compounds of the general formula (I), in which the variables are as defined in claim 1, the use of these compounds as pharmaceutical compositions, pharmaceutical compositions comprising the compounds and methods of treatment employing these compounds and compositions. The present compounds are useful in the treatment and/or prevention of conditions mediated by Peroxisome Proliferator-Activated Receptors (PPAR), in particular the PPAR? subtype, namely, type 1 diabetes, type 2 diabetes, dyslipidaemia, syndrome X (including the metabolic syndrome, i.e. impaired glucose tolerance, insulin resistance, hyper-triglyceridaemia and/or obesity), cardiovascular diseases (including atherosclerosis) and hypercholesterolaemia.
Type:
Application
Filed:
May 3, 2005
Publication date:
August 20, 2009
Applicant:
Novo Nordisk A/S
Inventors:
Miroslav Havranek, Per Sauerberg, Ingrid Pettersson, Pavel Pihera, Søren Ebdrup
Abstract: The present invention provides compositions and methods for treating otic disorders. More specifically, the present invention describes the use of agents that down-regulate expression of Tanis and/or p21Waf1/Cip1/Sd1 genes to treat such disorders of the ear.
Abstract: Disclosed are fenofibric acid amorphous dispersions containing amorphous fenofibric acid and an amorphous dispersion excipient. The amorphous dispersions can be prepared by e.g., spray drying techniques and formulated into pharmaceutical products.
Type:
Application
Filed:
December 16, 2008
Publication date:
July 16, 2009
Inventors:
Tong Sun, Shawn Watson, Heidi A. Pazamickas, Joseph Forth
Abstract: This invention relates to the use of fenofibrate or a derivative thereof for the manufacture of a medicament for the prevention and/or treatment of retinopathy.
Abstract: Agents useful for the treatment of various metabolic disorders, such as insulin resistance syndrome, diabetes, polycystic ovary syndrome, hyperlipidemia, fatty liver disease, cachexia, obesity, atherosclerosis and arteriosclerosis are disclosed, compound of the formula (I): wherein n is 1 or 2; m is 0, 1, 2, 3, 4, 5, 6, 7 or 8; q is 0 or 1; t is 0 or 1; R1 is alkyl having from 1 to 3 carbon atoms; R2 is hydrogen, halo, alkyl having from 1 to 3 carbon atoms, or alkoxy having from 1 to 3 carbon atoms; R3 and R4 together are alkyl having two or three carbon atoms; or R3 and R4 are the same as each other and each is methyl or ethyl; R5 is hydrogen or alkyl having from one to six carbon atoms.
Abstract: This invention relates to the use of a group of aryl ureas in treating cytokine mediated diseases and proteolytic enzyme mediated diseases, and pharmaceutical compositions for use in such therapy.
Type:
Grant
Filed:
February 1, 2002
Date of Patent:
April 14, 2009
Assignee:
Bayer Pharmaceuticals Corporation
Inventors:
Scott Miller, Martin Osterhout, Jacques Dumas, Uday Khire, Timothy B. Lowinger, William J. Scott, Roger A. Smith, Jill E. Wood, David E. Gunn, Holia Hatoum-Mokdad, Marell Rodriguez, Robert Sibley, Ming Wang, Tiffany Turner, Catherine Brennan
Abstract: Novel compounds of the general formula (I), the use of these compounds as pharmaceutical compositions, pharmaceutical compositions comprising the compounds and methods of treatment employing these compounds and compositions. The present compounds are activators of PPAR? and should be useful for treating conditions mediated by the same.
Type:
Application
Filed:
December 21, 2006
Publication date:
April 9, 2009
Inventors:
Per Sauerberg, Pavel Pihera, Zdenek Polivka, Miroslav Havranek, Ingrid Pettersson, John Patrick Mogensen
Abstract: Compounds that reduce serum retinol levels are used to treat ophthalmic conditions associated with the overproduction of waste products that accumulate during the course of the visual cycle. We describe methods, compounds, and compositions to treat, for example, the macular degenerations and dystrophies or to alleviate symptoms associated with such ophthalmic conditions.
Type:
Application
Filed:
September 15, 2008
Publication date:
April 2, 2009
Applicant:
SIRION THERAPEUTICS, INC.
Inventors:
Nathan L. MATA, Kim B. PHAN, Tam V. BUI, Mustapha HADDACH
Abstract: A transdermal active principle delivery means comprises a skin adherent or otherwise skin-tolerant substrate applicable to a skin area affected by DNA virus, which substrate includes a composition for treating DNA comprising a transdermally effective carrier medium including at least one active principle selected from the group consisting of diuretic agents and/or cardiac glycoside agents.
Abstract: Methods for treating diabetes by increasing the insulin secretion by administration of a GLP-1 receptor agonist and/or a DPP-IV inhibitor in combination with a proton pump inhibitor and optionally a PPAR agonist are provided.
Type:
Application
Filed:
June 23, 2005
Publication date:
February 12, 2009
Applicant:
Novo Nordisk A/S
Inventors:
Jacob Sten Petersen, Lars Hansen, Elisabeth D. Galsgaard
Abstract: The present invention provides compositions and methods for treating glaucoma, methods for diagnosing glaucoma, and methods for identifying agents which may be useful in the treatment of glaucoma. More specifically, the present invention describes the use of agents that modulate the expression of serum amyloid A.
Type:
Application
Filed:
February 27, 2008
Publication date:
February 5, 2009
Applicant:
ALCON, INC.
Inventors:
Abbot F. CLARK, Wan-Heng WANG, Loretta MCNATT
Abstract: The present invention is directed to novel, potent, and selective agents, which are agonists or antagonists of the one or more of the individual receptors of the S1P receptor family. The compounds of the invention are useful as therapeutics for treating medical conditions associated with agonism or antagonism of the individual receptors of the S1P receptor family.
Type:
Application
Filed:
March 11, 2008
Publication date:
January 29, 2009
Inventors:
Grier A. Wallace, Eric C. Breinlinger, Kevin P. Cusack, Shannon R. Fix-Stenzel, Thomas D. Gordon, Adrian D. Hobson, Martin E. Hayes, Graham K. Ansell, Pintipa Grongsaard
Abstract: Embodiments of the present invention are related to novel therapeutic drugs, drug combinations, and associated methods for treating or preventing pulmonary disease, including pulmonary hypertension, pulmonary fibrosis, asthma and COPD, and heart failure, together with other pulmonary and cardiovascular diseases and their complications. More particularly, aspects of the present invention are related to the use of cicletanine and ruboxistaurin as monotherapies or in combination with other agents for treatment of disease. Cicletanine may be used as pure (+) or (?) enantiomers or as a racemic or non-racemic mixture of those enantiomers.
Type:
Application
Filed:
January 3, 2008
Publication date:
December 18, 2008
Applicant:
Gilead Sciences, Inc.
Inventors:
Glenn V. Cornett, James Page, Wayne A. Jones, Karen Page
Abstract: Compounds of the formula (I): in which R, R1, R2 and R3 are as defined in the description, to their use for the treatment of dyslipidaemia, atherosclerosis and diabetes, to pharmaceutical compositions comprising them and to the processes for the preparation of these compounds.
Type:
Grant
Filed:
April 6, 2005
Date of Patent:
December 16, 2008
Assignee:
Merck Patent GmbH
Inventors:
Jean Jacques Zeiller, Hervè Dumas, Valérie Guyard-Dangremont, Isabelle Berard, Francis Contard, Daniel Guerrier, Gérard Ferrand, Yves Bonhomme
Abstract: Compounds having a formula: or a pharmaceutically acceptable salt or prodrug thereof, are provided, and are useful for the treatment of metabolic disorders.
Abstract: The present invention relates to a method for lowering serum lipids, eg. triglycerides and/or cholesterol in a subject comprising administering a GLP-1 agonist to said subject.
Type:
Application
Filed:
August 22, 2007
Publication date:
November 13, 2008
Applicant:
Novo Nordisk A/S
Inventors:
Liselotte Bjerre Knudsen, Johan Selmer, Jeppe Sturise, Philip Just Larsen
Abstract: The invention relates to novel compounds of general formula I wherein M represents hydrogen, or a metallic cation, preferably an alkaline metal, or alkaline-earth metal, and n is equal to 1, 2 or 3. The present invention also comprises compounds of general formula I in their equilibrium forms, including lactonic forms, their enantiomers in pure form, or in an enriched form in one of the optical isomers, racemic mixtures, diastereomers and solvates thereof. The present invention further relates to processes for the preparation of compounds of general formula I, to pharmaceutical compositions comprising compounds of general formula I as only active ingredient, or in association with other active ingredients. Another aspect of the invention is the use of compounds of general formula I for the treatment of dyslipidemia, associated, or not, to other metabolic disorders, such as glucose intolerance syndrome and type 1 or 2 diabetes mellitus, by means of isolated administration or combined with other substances.
Type:
Application
Filed:
November 15, 2006
Publication date:
November 13, 2008
Inventors:
Jorge Ruas Da Silva, Ana Maria Staack Reis Machado, Joaquim Alberto Barros Pereira, Joao Carlos Ramos Damil, Carlos Alberto Casimiro Caixado, Augusto Eugenio Pardal Filipe
Abstract: The present invention describes methods for using Treprostinil or its derivative, or a pharmaceutically acceptable salt thereof, for the treatment and/or prevention of interstitial lung disease or asthma, or a condition, such as pulmonary fibrosis, associated with interstitial lung disease or a condition associated with asthma. The invention also relates to kits for treatment and/or prevention of such condition that include an effective amount of Treprostinil or its derivative, or a pharmaceutically acceptable salt thereof.
Type:
Application
Filed:
February 8, 2008
Publication date:
November 13, 2008
Inventors:
Michael Wade, Stuart Rich, Eugene Sullivan, Robert Roscigno, Roger Jeffs
Abstract: There are provided according to the invention compounds of formula (I) in free or salt form, wherein R<1>, R<2>, R<3>, X, Y, Z, m, and n are as described in the specification, process for preparing them, and their use as pharmaceuticals.
Type:
Application
Filed:
May 3, 2005
Publication date:
October 30, 2008
Inventors:
David Andrew Sandham, Katharine Louise Turner, Catherine Leblanc
Abstract: The invention features 4-((phenoxyalkyl)thio)-phenoxyacetic acids and analogs, compositions containing them, and methods of using them as PPAR modulators to treat or inhibit the progression of, for example, dyslipidemia.
Type:
Application
Filed:
June 23, 2008
Publication date:
October 30, 2008
Inventors:
Gee-Hong Kuo, Rui Zhang, Aihua Wang, Alan DeAngelis, Keith Demarest, Patricia Pelton
Abstract: Compounds, compositions, and methods of avoiding edema while treating or preventing PPAR?-mediated diseases, including cancer, using derivatives and prodrugs are provided.