Abstract: Disclosed are methods of modulating a stress activated protein kinase (SAPK) system with an active compound, wherein the active compound exhibits low potency for inhibition of at least one p38 MAPK; and wherein the contacting is conducted at a SAPK-modulating concentration that is at a low percentage inhibitory concentration for inhibition of the at least one p38 MAPK by the compound. Also disclosed are derivatives of pirfenidone. These derivatives can modulate a stress activated protein kinase (SAPK) system.
Type:
Application
Filed:
June 20, 2012
Publication date:
October 11, 2012
Applicant:
INTERMUNE, INC.
Inventors:
Lawrence M. Blatt, Scott D. Seiwert, Leonid Beigelman, Ramachandran Radhakrishnan, Karl Kossen, Vladimir Serebryany
Abstract: Compounds having the formula I wherein R1, R2, R3, R4a, R4b, R4c, R5, R6, R9 and n are as defined herein are Hepatitis C virus NS5b polymerase inhibitors. Also disclosed are compositions and methods for treating an HCV infection and inhibiting HCV replication.
Type:
Grant
Filed:
July 22, 2009
Date of Patent:
September 25, 2012
Assignee:
Roche Palo Alto LLC
Inventors:
Kenneth Albert Brameld, David Scott Carter, Elbert Chin, Javier de Vicente Fidalgo, Jim Li, Ryan Craig Schoenfeld, Eric Brian Sjogren, Francisco Xavier Talamas
Abstract: The present invention relates to novel compounds, in particular novel pyridinone derivatives according to Formula (I) wherein all radicals are as defined in the application and claims. The compounds according to the invention are positive allosteric modulators of metabotropic receptors—subtype 2 (“mGluR2”) which are useful for the treatment or prevention of neurological and psychiatric disorders associated with glutamate dysfunction and diseases in which the mGluR2 subtype of metabotropic receptors is involved. In particular, such diseases are central nervous system disorders selected from the group of anxiety, schizophrenia, migraine, depression, and epilepsy. The invention is also directed to pharmaceutical compositions and processes to prepare such compounds and compositions, as well as to the use of such compounds for the prevention and treatment of such diseases in which mGluR2 is involved.
Inventors:
Jose Maria Cid-Nunez, Andres Avelino Trabanco-Suarez, Gregor James MacDonald, Guillaume Albert Jacques Duvey, Robert Johannes Lutjens, Patrick Terry Finn
Abstract: Compounds of the formula: are described wherein: A1 is ascorbic acid, dehydroascorbic acid, ascorbyl-2-phosphate, an analog thereof, or a salt thereof; L is a linking group coupled to A1 at the C5 or C6 position thereof; and B1 is an active agent such as an imaging agent or therapeutic agent (e.g. a bisphosphonate), along with pharmaceutically acceptable salts and prodrugs thereof. The compounds are useful for, among other things, improving cartilage uptake of active agents administered for joint diseases such as osteoarthritis and rheumatoid arthritis, and for improving gastrointestinal absorption of bisphosphonates.
Type:
Grant
Filed:
April 21, 2006
Date of Patent:
August 21, 2012
Assignee:
Duke University
Inventors:
Virginia Byers Kraus, Amy Lynn McNulty, Eric John Toone
Abstract: The present invention is related to N-hydroxyamide derivatives of Formula (I) and use thereof in particular for the treatment and/or prophylaxis of autoimmune disorders, inflammatory diseases, cardiovascular diseases, neurodegenerative diseases, cancer, respiratory diseases and fibrosis, including multiple sclerosis, arthritis, emphysema, chronic obstructive pulmonary disease, liver and pulmonary fibrosis.
Abstract: The invention provides a tobacco composition for use in a smoking article or a smokeless tobacco composition that comprises an extract derived from a component of a plant of the Nicotiana species. The invention also provides smoking articles and smokeless tobacco compositions that include the extracts described herein, and methods for preparing extracts derived from a component of a plant of the Nicotiana species for addition to a tobacco composition.
Type:
Application
Filed:
January 28, 2011
Publication date:
August 2, 2012
Inventors:
Michael Francis Dube, William Monroe Coleman, III
Abstract: Crystalline pyridone compound, which is the white needle crystal containing no water and other crystallization solvents. Its unit cell belongs to monoclinic system and has space group of P21/n, wherein a=3.8512(2), b=20.2535(12), c=12.1628(6) ?, ?=92.850(5)° and crystal cell volume V=947.53(9) ?3. Pyridone compound crystal of this form has the needed properties for preparing or making treatment compositions in large scale. It can be used for treating organs fibrosis of liver, kidney, lung and etc. and reducing skin scars.
Abstract: The present invention relates to a compound of formula I, in all its isomeric forms and pharmaceutically acceptable salts thereof, their manufacture, pharmaceutical compositions containing them and their use as medicaments for the treatment and/or prophylaxis of diseases which can be treated with HDL-cholesterol raising agents, such as dyslipidemia, atherosclerosis and cardiovascular diseases.
Abstract: A tablet characterized by comprising 5-methyl-1-phenyl-2-(1H)-pyridone as the main ingredient and, based on the main ingredient, 10 to 50 wt. % excipient, 5 to 40 wt. % disintegrator, 1 to 10 wt. % binder, 0.5 to 5 wt. % lubricant, 2 to 6 wt. % coating basis, and 0.05 to 3 wt. % light-shielding agent, wherein the odor or bitterness of the 5-methyl-1-phenyl-2-(1H)-pyridone is masked and the light stability is improved.
Abstract: This invention relates to a bipolar antimicrobial particle for use in laundry detergent compositions, fabric conditioners, personal care and cosmetic compositions and a process for making the same. In view of the foregoing, it is an object of the present invention to provide a stabile antimicrobial agent immobilised on a carrier particle. It is a further objective to provide an antimicrobial particle with improved retention to the fabric so that larger amounts of antimicrobial will be available even after rinsing. Surprisingly it has been found that antimicrobial molecules tagged by surface reaction onto naturally occurring asymmetric clay surfaces, act as an antimicrobial particle with improved retention properties with improved stability.
Abstract: The present invention relates to compounds useful in therapy, in particular in the treatment of psychosis, to compositions comprising said compounds, and to methods of treating diseases comprising the administration of said compounds.
Type:
Grant
Filed:
December 14, 2010
Date of Patent:
June 26, 2012
Assignee:
H. Lundbeck A/S
Inventors:
Nikolay Khanzhin, Søren Møller Nielsen, Karsten Juhl, Lars Kyhn Rasmussen
Abstract: The invention relates to substituted nicotinamides, to processes for their preparation, to medicaments comprising these compounds and to the use of these compounds in the preparation of medicaments.
Type:
Grant
Filed:
March 10, 2010
Date of Patent:
May 15, 2012
Assignee:
Gruenenthal GmbH
Inventors:
Sven Kühnert, Beatrix Merla, Gregor Bahrenberg, Wolfgang Schröder
Abstract: Compounds of formula (I) and salts thereof are provided: wherein n is 0, 1, 2 or 3; R1 is selected from phenyl and pyridyl, each of which is optionally substituted by one or two groups independently selected from C1-4alkyl and halogen; and R2 is selected from H and CH3 when n is 1 and R2 is H when n is 2 or 3. Processes for preparation, pharmaceutical compositions, and uses thereof as a medicament, for example in the treatment of a disease or condition mediated by a reduction or imbalance in glutamate receptor function, such as schizophrenia or cognition impairment, are also disclosed.
Type:
Grant
Filed:
December 17, 2008
Date of Patent:
May 8, 2012
Assignee:
Glaxo Group Limited
Inventors:
Nicolas Bertheleme, Wai Ngor Chan, Jaqueline Sandra Scott, Simon E. Ward
Abstract: Compounds having the formula I wherein R1, R2, R3, R4, R5a, R5b, R5c and R6 are as defined herein are Hepatitis C virus NS5b polymerase inhibitors. Also disclosed are compositions and methods for treating an HCV infection and inhibiting HCV replication.
Type:
Grant
Filed:
April 23, 2010
Date of Patent:
April 17, 2012
Assignee:
Roche Palo Alto LLC
Inventors:
Eun Kyung Lee, Ryan Craig Schoenfeld, Francisco Xavier Talamas
Abstract: Compounds of the formula I: or pharmaceutically acceptable salts thereof, wherein m, n, R1, R2, R3, R4 and R5 are as defined herein. Also disclosed are methods of making the compounds and using the compounds for treatment of diseases associated with the P2X7 purinergic receptor.
Type:
Grant
Filed:
December 14, 2009
Date of Patent:
April 10, 2012
Assignee:
Roche Palo Alto LLC
Inventors:
Francisco Javier Lopez-Tapia, Keith Adrian Murray Walker, Shu-Hai Zhao
Abstract: The present invention relates to compounds of formula I wherein R.sup.1a to R.sup.1e and R.sup.2 to R.sup.5 are as defined in the description and claims, and pharmaceutically acceptable salts thereof. The compounds are glucocorticoid receptor antagonists useful for the treatment and/or prevention of diseases such as diabetes, dyslipidemia, obesity, hypertension, cardiovascular diseases, adrenal imbalance or depression.
Type:
Grant
Filed:
March 19, 2010
Date of Patent:
March 20, 2012
Assignee:
Hoffman-La Roche Inc.
Inventors:
Daniel Hunziker, Chrisitan Lerner, Werner Mueller, Ulrike Obst Sander, Philippe Pflieger, Pius Waldmeier
Abstract: This invention relates to a series of substituted cyclohexane containing analogues which are agonists of GPR119 intended to treat metabolic diseases mediated by GPR119 including Type I & II diabetes mellitus. Diabetes mellitus is an ever-increasing threat to human health causing various complications (blindness, kidney failure, neuropathy, heart attack, stroke, etc.). Recently it was found that activation of GPR119 which is highly expressed in pancreatic beta cells causes glucose dependent insulin secretion and GLP-1 release. Many pharmaceuticals are currently developing GPR119 agonists and herein we disclose alternative GPR119 agonists. Our invention describes GPR119 agonists having structural Formula (I), pharmaceutically acceptable salt or solvate of Formula (I), isomer or prodrug of Formula (I), and combination therapy of Formula (I) with other anti-diabetic drugs like DPP-IV inhibitors and/or insulin sensitizers.
Type:
Application
Filed:
March 17, 2011
Publication date:
March 1, 2012
Applicant:
CHEMIZON, A DIVISION OF OPTOMAGIC CO., LTD.
Inventors:
Sang Uk Kang, Min Jeong Kim, Byung Nam Kang, Wei Tan, Albert Charles Gyorkos, Suk Young Cho
Abstract: The invention is concerned with the compounds of formula I: and pharmaceutically acceptable salts and esters thereof, wherein X, Q, and R1-R6 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.
Type:
Grant
Filed:
November 9, 2009
Date of Patent:
February 28, 2012
Assignee:
Hoffmann-La Roche Inc.
Inventors:
Fariborz Firooznia, Paul Gillespie, Tai-An Lin, Eric Mertz, Achyutharao Sidduri, Sung-Sau So, Jenny Tan, Kshitij Chhabilbhai Thakkar
Abstract: This invention relates to new aryl ureas and methods for their synthesis. The inventive compounds are useful in the treatment of (i) raf mediated diseases, for example, cancer, (ii) p38 mediated diseases such as inflammation and osteoporosis, and (iii) VEGF mediated diseases such as angiogenesis disorders.
Type:
Grant
Filed:
February 11, 2003
Date of Patent:
February 7, 2012
Assignee:
Bayer Healthcare LLC
Inventors:
Jacques Dumas, William J. Scott, Bernd Riedl, Du-Schieng Chien, Ala Nassar, Wendy Lee, Susan Bjorge, Laszlo Musza
Abstract: Provided herein are hydroxypyridone derivatives, for example, a compound of Formula I, and pharmaceutical compositions thereof. Also provided herein are methods of their use for treating, preventing, or ameliorating one or more symptoms of a proliferative disease.
Abstract: A process for synthesizing pirfenidone from bromobenzene having less than about 0.15% by weight dibromobenze is disclosed. Also disclosed are processes of synthesizing pirfenidone without using ethyl acetate or n-butanol, and pirfenidone having controlled levels of ethyl acetate, n-butanol, di(5-methyl-2-pyridinone)benzenes, and other impurities having specified retention times. Also disclosed are formulated dosage forms including the disclosed pirfenidone.
Type:
Application
Filed:
September 26, 2011
Publication date:
January 19, 2012
Applicant:
INTERMUNE, INC.
Inventors:
Sabine M. Pyles, Michael Cyr, Ramachandran Radhakrishnan
Abstract: Novel cyclohexyl-1,4-diamine compounds corresponding to formula I, processes for the production thereof, pharmaceutical compositions containing these compounds, methods of producing pharmaceutical compositions including these compounds and related methods of treating or inhibiting certain diseases or conditions.
Abstract: A pyridone derivative represented by Formula [1] or an agriculturally acceptable salt thereof: wherein R1 is a C1-6 alkyl group, a C2-6 alkenyl group, a C2-6 alkynyl group, or the like; R2 and R3 are each independently a hydrogen atom, a nitro group, a cyano group, or the like; and A is a group represented by Formula A-1, Formula A-2, Formula A-3, Formula A-4, or Formula A-5: The compounds represented by general formula [1] control various weeds growing in upland fields, orchards, paddy fields, and non-crop lands while showing high safety to useful plants and crops.
Type:
Grant
Filed:
January 31, 2007
Date of Patent:
December 13, 2011
Assignees:
Kumiai Chemical Industry Co., Ltd., Ihara Chemical Industry Co., Ltd.
Abstract: This invention relates to urea compounds containing a pyridine, quinoline, or isoquinoline functionality which is oxidized at the nitrogen heteroatom and which are useful in the treatment of (i) raf mediated diseases, for example, cancer, (ii) p38 mediated diseases such as inflammation and osteoporosis, and (iii) VEGF mediated diseases such as angiogenesis disorders.
Type:
Grant
Filed:
January 25, 2010
Date of Patent:
December 6, 2011
Assignee:
Bayer Healthcare LLC
Inventors:
Jacques Dumas, William J. Scott, Bernd Riedl
Abstract: Described herein are compounds that are antagonists of PGD2 receptors. Also described are pharmaceutical compositions that include the compounds described herein, and methods of using such antagonists of PGD2 receptors, alone or in combination with other compounds, for treating respiratory, cardiovascular, and other PGD2-dependent or PGD2-mediated conditions or diseases.
Type:
Grant
Filed:
September 28, 2009
Date of Patent:
November 1, 2011
Assignee:
Panmira Pharmaceuticals, LLC
Inventors:
John Howard Hutchinson, Nicholas Simon Stock, Jeffrey Roger Roppe, Jill Melissa Scott, Brian Andrew Stearns, Yen Pham Truong, Deborah Volkots, Timothy Parr
Abstract: The invention relates to the field of medicine, namely to new biologically active compounds, particularly to 2,4,6-trimethyl-3-hydroxypyridine derivatives and salts thereof (compound 1) having antioxidant, geroprotective and anti-ischemic action. The salts of compound (1) are prepared by reacting equimolecular quantities of 2,4,6-trimethyl-3-hydroxypyridine and dicarboxylic in solution of a lower alcohol at a temperature of 60-100° C. with following treatment of the reaction mass with an organic solvent and maintaining for 2-5 h at 10-15 ° C.
Type:
Grant
Filed:
December 18, 2008
Date of Patent:
October 25, 2011
Assignee:
Marvel Lifesciences Limited
Inventors:
Leonid Dmitrievich Smirnov, Larisa Kasimirovna Smirnova, legal representative, Michail Arkadievich Ostrovsky, Aleksey Michailovich Sipyagin, Natalia Y. Sipyagina, legal representative, Nadezda A. Sipyagina, legal representative, Aleksandr Evgenievich Doncov
Abstract: The present application relates to calcium channel inhibitors containing compounds of formula (I) wherein Ar1, Ar2, L1, L2, n, R1, R4, X and Y are as defined in the specification. The present application also relates to compositions comprising such compounds, and methods of treating conditions and disorders using such compounds and compositions.
Type:
Grant
Filed:
October 1, 2009
Date of Patent:
October 25, 2011
Assignees:
Abbott Laboratories, Abbott GmbH & Co. KG
Inventors:
Pramila A. Bhatia, George A. Doherty, Irene Drizin, Helmut Mack, Richard J. Perner, Andrew O. Stewart, Qingwei Zhang
Abstract: Diaryl ethers in which one of the aryl groups is a phenyl fused to a cycloalkyl or heterocyclic ring, to which is attached an acetic acid group, are agonists of G-protein coupled receptor 40 (GPR40) and are useful as therapeutic compounds, particularly in the treatment of Type 2 diabetes mellitus, and of conditions that often accompany this disease, including insulin resistance, obesity and lipid disorders.
Type:
Grant
Filed:
October 26, 2007
Date of Patent:
October 18, 2011
Assignee:
Merck Sharp & Dohme Corp.
Inventors:
Min Ge, Songnian Lin, Shawn P. Walsh, Lihu Yang, Changyou Zhou
Abstract: Compounds and methods of treating anti-inflammatory conditions are disclosed.
Type:
Grant
Filed:
March 5, 2009
Date of Patent:
October 18, 2011
Assignee:
Anacor Pharmaceuticals, Inc.
Inventors:
Tsutomu Akama, Yong-Kang Zhang, Charles Z. Ding, Jacob J. Plattner, Kirk R. Maples, Yvonne Freund, Virginia Sanders, Yi Xia, Stephen J. Baker, James A. Nieman, Xiaosong Lu, Marcelo Sales, Rashmi Sharma, Rajeshwar Singh, Robert Jacobs, Daitao Chen, Michael Richard Kevin Alley
Abstract: To provide a method for producing a specific nicotinic acid derivative or a salt thereof. A method for producing a nicotinic acid derivative represented by the formula (I): wherein each of X1 and X2 which are independent of each other, is a hydrogen atom, a halogen atom, an alkyl group, an alkoxy group, a haloalkyl group or a haloalkoxy group; R is an alkyl group; and Hal is a chlorine atom or a bromine atom; or a salt thereof, is provided which comprises reacting a compound represented by the formula (II): is wherein X1, X2 and R are as defined above, or a salt thereof, with a halogenating agent.
Abstract: A method of treating a malignant tumor selected from the group consisting of leukemia, colorectal cancer, ovarian cancer, oral cancer, lung carcinoma, breast carcinoma, prostate carcinoma, and melanoma by administering to a patient in need thereof an effective amount of at least one compound represented by formula (1) wherein A, X, Q, R1-3, and n are defined herein.
Abstract: Compounds of the invention, such as compounds of formula (I): where n, m, A, B, R1, R2, R3, R4 and R5 are defined herein, are useful as modulators of the activity of liver X receptors. Pharmaceutical compositions containing the compounds and methods of using the compounds are also disclosed.
Type:
Grant
Filed:
December 17, 2008
Date of Patent:
September 6, 2011
Assignee:
Exelixis, Inc.
Inventors:
Christopher D. Bayne, Alan T. Johnson, Shao Po Lu, Raju Mohan, Michael C. Nyman, Edwin J. Schweiger, William C. Stevens, Jr., Haixia Wang, Yinong Xie
Abstract: Described herein are solid, stable pharmaceutical formulations of cannabinoid receptor inverse agonists, such as taranabant, and processes of making such formulations. Additionally, described herein are solid stable pharmaceutical formulations of cannabiniod inverse agonists, such as taranabant, and an additional therapeutic agent, as well as processes for making such pharmaceutical formulations.
Type:
Grant
Filed:
April 17, 2009
Date of Patent:
August 23, 2011
Assignee:
Merck Sharp & Dohme Corp.
Inventors:
Craig McKelvey, Sarah Geers, Justin Moser, Bhagwant Rege, Dina Zhang, Sutthilug Sotthivirat
Abstract: Compounds of formula (I) wherein R1-R5, n and m have the same meaning as given in the description, having cooling properties are disclosed. Furthermore a process of their production and consumer products comprising them are disclosed.
Type:
Application
Filed:
December 4, 2008
Publication date:
July 28, 2011
Inventors:
Stefan Michael Furrer, Thomas Scott McCluskey
Abstract: The present invention provides compounds of formula I wherein Ring A, Ring B, m, Rx, Ry, W and R1 are as defined herein, pharmaceutically acceptable salts and compositions thereof, and methods of using the same.
Type:
Grant
Filed:
October 17, 2008
Date of Patent:
July 19, 2011
Assignee:
Avila Therapeutics, Inc.
Inventors:
Juswinder Singh, Shomir Ghosh, Arthur F. Kluge, Russell C. Petter, Richland W. Tester
Abstract: Ambient-temperature molten salts of formula (I): wherein Y+ is a cation selected from the group consisting of an ammonium ion, a sulfonium ion, a pyridinium ion, a(n) (iso)thiazolium ion, and a(n) (iso)oxazolium ion that may be optionally substituted with C1-10 alkyl and/or C1-10 alkyl having ether linkage, provided that the above cation has at least one substituent of —CH2Rf1 or —OCH2Rf1 (wherein Rf1 is C1-10 perfluoroalkyl); Rf2 and Rf3 are independently C1-10 perfluoroalkyl or may together form C1-4 perfluoroalkylene; and X is —SO2— or —CO—.
Abstract: The present invention provides a compound of formula I: wherein R1, R2, R3, R4, and R5 are as defined herein. The present invention also provides pharmaceutical compositions and methods using such compositions for treating a caspase-mediated diseases and processes for preparing the compounds of the invention.
Type:
Grant
Filed:
June 17, 2008
Date of Patent:
June 14, 2011
Assignee:
Vertex Pharmaceutical Incoporated
Inventors:
Guy Brenchley, Jean-Damien Charrier, Steven Durrant, Ronald Knegtel, Michael Mortimore, John Studley
Abstract: The present invention provides a novel compound having an excellent AMPA receptor inhibitory action and/or kainate inhibitory action. A compound represented by the following formula, a salt thereof or hydrates thereof. In the formula, Q indicates NH, O or S; and R1, R2, R3, R4 and R5 are the same as or different from each other and each indicates hydrogen atom, a halogen atom, a C1-6 alkyl group or a group represented by the formula —X-A (wherein X indicates a single bond, an optionally substituted C1-6 alkylene group etc.; and A indicates an optionally substituted C6-14 aromatic hydrocarbocyclic group or 5- to 14-membered aromatic heterocyclic group etc.).
Type:
Grant
Filed:
February 27, 2009
Date of Patent:
May 10, 2011
Assignee:
Eisai R&D Management Co., Ltd.
Inventors:
Satoshi Nagato, Kohshi Ueno, Koki Kawano, Yoshihiko Norimine, Koichi Ito
Abstract: A tablet characterized by comprising 5-methyl-1-phenyl-2-(1H)-pyridone as the main ingredient and, based on the main ingredient, 10 to 50 wt. % excipient, 5 to 40 wt. % disintegrator, 1 to 10 wt. % binder, 0.5 to 5 wt. % lubricant, 2 to 6 wt. % coating basis, and 0.05 to 3 wt. % light-shielding agent, wherein the odor or bitterness of the 5-methyl-1-phenyl-2-(1H)-pyridone is masked and the light stability is improved.
Abstract: The present invention relates to the use of compounds which have the following general formula (I), wherein R1 and R2 are independently selected from optionally substituted aryl, optionally substituted C1 to C12 alkyl and H; and R3 and R4 are independently selected from hydroxy, optionally substituted C1 to C6 alkyl, optionally substituted phenyl and H, in a method of preventing or reducing fouling, particularly in the marine environment. The compounds of the present invention have the considerable advantage of providing the antifouling coating market with an organic alternative to the existing technology which relies heavily on the addition of copper to obtain significant antifouling effects. The compounds we have developed may be used as cheap, easy to prepare additives that do not contain metals and therefore have reduced toxicity in marine environment.
Type:
Application
Filed:
May 18, 2009
Publication date:
April 21, 2011
Applicants:
NATIONAL UNIVERSITY OF SINGAPORE, AGENCY FOR SCIENCE, TECHNOLOGY AND RESEARCH, MARITIME AND PORT AUTHORITY OF SINGAPORE
Inventors:
Lay Ming Serena Teo, Daniel Rittschof, Felicity Jameson, Christina Chai, Chia Lung Chen, Siew Chen Serina Lee
Abstract: The present invention relates to organic molecules capable of modulating tyrosine kinase signal transduction in order to regulate, modulate and/or inhibit abnormal cell proliferation.
Type:
Grant
Filed:
November 16, 2007
Date of Patent:
March 29, 2011
Assignee:
Allergan, Inc.
Inventors:
Julie A. Wurster, Clarence Eugene Hull, III, Richard C. Yee, Sougato Boral, Shimiao Wang, Thomas C. Malone
Abstract: The present invention provides compounds of formula (I), or pharmaceutically acceptable salts or solvates thereof, methods for their preparation, methods for their use, and pharmaceutical formulations comprising them.
Type:
Grant
Filed:
January 9, 2007
Date of Patent:
January 11, 2011
Assignee:
Pfizer Inc.
Inventors:
Mitchell David Nambu, Leena Bharat Kumar Patel, Brian Douglas Patterson, Sylvie Kim Sakata, John Howard Tatlock
Abstract: Crystalline pyridone compound, which is the white needle crystal containing no water and other crystallization solvents. Its unit cell belongs to monoclinic system and has space group of P21/n, wherein a=3.8512(2), b=20.2535(12), c=12.1628(6) ?, ?=92.850(5)° and crystal cell volume V=947.53(9) ?3. Pyridone compound crystal of this form has the needed properties for preparing or making treatment compositions in large scale. It can be used for treating organs fibrosis of liver, kidney, lung and etc. and reducing skin scars.
Abstract: A process for synthesizing pirfenidone from bromobenzene having less than about 0.15% by weight dibromobenzene is disclosed. Also disclosed are processes of synthesizing pirfenidone without using ethyl acetate or n-butanol, and pirfenidone having controlled levels of ethyl acetate, n-butanol, di(5-methyl-2-pyridinone)benzenes, and other impurities having specified retention times. Also disclosed are formulated dosage forms including the disclosed pirfenidone.
Type:
Application
Filed:
June 2, 2010
Publication date:
January 6, 2011
Applicant:
INTERMUNE, INC.
Inventors:
Sabine M. Pyles, Michael Cyr, Ramachandran Radhakrishnan