Benzothiazines (including Hydrogenated) Patents (Class 544/49)
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Patent number: 10995043Abstract: Provided is a method for producing a perfluoroalkylated compound at low cost, safely and with high efficiency. A method for producing a perfluoroalkylated compound, comprising reacting a bis(perfluoroalkanoyl) peroxide with a compound having a carbon-carbon unsaturated bond and/or an aromatic ring having a hydrogen atom bonded thereto in the presence of a copper catalyst.Type: GrantFiled: December 12, 2016Date of Patent: May 4, 2021Assignee: RikenInventors: Mikiko Sodeoka, Shintaro Kawamura
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Patent number: 9487474Abstract: The present invention relates to compounds having the general Formula I: which absorb UV radiations and protect biological materials as well as non-biological materials from damaging exposure to UV radiations. The present invention also relates to formulations and compositions comprising such compounds for use in absorbing UV radiations and in protecting biological materials as well as non-biological materials against UV radiations.Type: GrantFiled: May 31, 2013Date of Patent: November 8, 2016Assignee: Elkimia, Inc.Inventors: Elie Abou-Khalil, Stephane Raeppel, Franck Raeppel
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Publication number: 20150111857Abstract: Compounds and compositions useful for treating disorders related to KIT and PDFGR are described herein.Type: ApplicationFiled: October 17, 2014Publication date: April 23, 2015Applicant: BLUEPRINT MEDICINES CORPORATIONInventors: Brian L. Hodous, Joseph L. Kim, Chandrasekhar V. Miduturu, Douglas Wilson, Yulian Zhang
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Patent number: 8940271Abstract: The invention includes compositions for transmucosal administration to an animal comprising at least one active agent and a pharmaceutically acceptable carrier. A preferred active agent is selected from the group consisting of meloxicam, carprofen, enrofloxacin, clemastine, diphenhydramine, digoxin, levothyroxine, cyclosporine, ondansetron, lysine, zolpidem, propofol, nitenpyram, ivermectin, milbemycin, and pharmaceutically acceptable salts, solvates and esters thereof. In another embodiment, the invention includes methods of treating or preventing a condition in an animal comprising transmucosally administering a composition comprising a therapeutically or prophylactically effective amount of an active agent and a pharmaceutically acceptable carrier.Type: GrantFiled: December 15, 2011Date of Patent: January 27, 2015Assignee: Abbott LaboratoriesInventors: Mark C. Heit, Antonio M. Benitz, Dennis F. Steadman, David M. Petrick
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Patent number: 8822457Abstract: This application discloses 5-phenyl-1H-pyridin-2-one and 6-phenyl-2H-pyridazin-3-one derivatives according to generic Formulae I-IV: wherein, variables R, X, Y1, Y2, Y2?, Y3, Y4, n and m are defined as described herein, which inhibit Btk. The compounds disclosed herein are useful to modulate the activity of Btk and treat diseases associated with excessive Btk activity. The compounds are further useful to treat inflammatory and auto immune diseases associated with aberrant B-cell proliferation such as rheumatoid arthritis. Also disclosed are compositions comprising compounds of Formulae I-IV and at least one carrier, diluent or excipient.Type: GrantFiled: September 11, 2013Date of Patent: September 2, 2014Assignee: Roche Palo Alto LLCInventors: Nolan James Dewdney, Rama K. Kondru, Bradley E. Loe, Yan Lou, Joel McIntosh, Timothy D. Owens, Michael Soth
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Publication number: 20140194413Abstract: This application discloses 5-phenyl-1H-pyridin-2-one and 6-phenyl-2H-pyridazin-3-one derivatives according to generic Formulae I-IV: wherein, variables R, X, Y1, Y2, Y2?, Y3, Y4, n and m are defined as described herein, which inhibit Btk. The compounds disclosed herein are useful to modulate the activity of Btk and treat diseases associated with excessive Btk activity. The compounds are further useful to treat inflammatory and auto immune diseases associated with aberrant B-cell proliferation such as rheumatoid arthritis. Also disclosed are compositions comprising compounds of Formulae I-IV and at least one carrier, diluent or excipient.Type: ApplicationFiled: September 11, 2013Publication date: July 10, 2014Applicant: Roche Palo Alto LLCInventors: Nolan James Dewdney, Rama K. Kondru, Bradley E. Loe, Yan Lou, Joel McIntosh, Timothy D. Owens, Michael Soth
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Publication number: 20130338153Abstract: Provided herein are PAK inhibitors and methods of utilizing PAK inhibitors for the treatment of CNS disorders.Type: ApplicationFiled: June 10, 2011Publication date: December 19, 2013Applicant: AFRAXIS, INC.Inventors: David Campbell, Sergio G. Duron, Benedikt Vollrath, Warren Wade
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Publication number: 20130303524Abstract: The subject matter herein is directed to carbazole-containing sulfonamide derivatives and pharmaceutically acceptable salts or hydrates thereof of structural formula I wherein the variable R1, R2, R3, R4, R5, R6, R7, A, B, C, D, E, F, G, H, a, and b are accordingly described. Also provided are pharmaceutical compositions comprising the compounds of formula I to treat a Cry-mediated disease or disorder, such as diabetes, obesity, metabolic syndrome, Cushing's syndrome, and glaucoma.Type: ApplicationFiled: May 10, 2013Publication date: November 14, 2013Inventors: Ross Bersot, Paul Humphries
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Publication number: 20130303525Abstract: The present invention relates to a series of substituted compounds having the general formula (I), including their stereoisomers and/or their pharmaceutically acceptable salts. (I) Wherein A, m, R1s, R2, R3, R4 are as defined herein. This invention also relates to methods of making these compounds including intermediates. The compounds of this invention are effective at the kappa (?) opioid receptor (KOR) site. Therefore, the compounds of this invention are useful as pharmaceutical agents, especially in the treatment and/or prevention of a variety of central nervous system disorders (CNS), including but not limited to acute and chronic pain, and associated disorders, particularly functioning peripherally at the CNS.Type: ApplicationFiled: July 19, 2011Publication date: November 14, 2013Applicants: DR. REDDY'S LABORATORIES, INC., DR. REDDY;S LABORATORIES LTD.Inventors: Pradip Kumar Sasmal, Vamsee Krishna Chintakunta, Vijay Potluri, Ish Kumar Khanna, Ashok Tehim, Mahaboobi Jaleel, Thomas Hogberg, Oystein Rist, Lisbeth Elster, Thomas Michael Frimurer, Lars-Ole Gerlach
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Patent number: 8389512Abstract: The invention is directed to novel crystalline forms of meloxicam. These novel crystalline forms of meloxicam have improved bioavailability, an enhanced rate of dissolution and shorter time to Cmax in blood, as compared to pure meloxicam.Type: GrantFiled: February 17, 2012Date of Patent: March 5, 2013Assignee: Thar PharmaceuticalsInventors: Mazen Hanna, Ning Shan, Miranda L. Cheney, David R. Weyna
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Patent number: 8334316Abstract: The present invention provides substituted di-, tri-, tetra- and penta-sulfide compounds and compositions, and methods of using the same for the treatment and/or prevention of a cell proliferative disorder. The present invention also provides methods for preparing trisulfide compounds and compositions.Type: GrantFiled: February 9, 2009Date of Patent: December 18, 2012Assignee: ACEA Biosciences, Inc.Inventors: Xiao Xu, Haoyun An, Xiaobo Wang
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Publication number: 20120202756Abstract: The present invention relates to prodrugs of a wide variety of drugs and pharmaceutical compositions containing such prodrugs. Methods for minimizing locally mediated (from within the gut lumen) adverse gastrointestinal events associated with the underivatised drug and increasing the sustainment of plasma drug levels with the aforementioned prodrugs are also provided. Thus, the present invention relates to the use of prodrugs of a wide diversity of drugs (other than opioids) to transiently inactivate them and so reduce directly, locally mediated adverse gastrointestinal (GI) side-effects normally evident after administration of the parent compound. Additionally, such prodrugs may confer improved pharmacokinetics.Type: ApplicationFiled: October 5, 2011Publication date: August 9, 2012Inventors: Richard Franklin, Martin Quibell, Robert G. Tyson, Bernard T. Golding
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Publication number: 20120168335Abstract: The invention provides pharmaceutical compositions comprising a therapeutically effective amount of meloxicam, or a pharmaceutically acceptable salt thereof, wherein the pharmaceutical compositions are in the form of a fast disintegrating dosage form suitable for releasing meloxicam rapidly in the oral cavity. Also provided are processes for preparing a pharmaceutical composition of the invention. Further provided are methods of treating arthritis or pain in a subject in need thereof, the method comprising orally administering to the subject a therapeutically effective amount of a pharmaceutical composition according to the invention.Type: ApplicationFiled: August 31, 2010Publication date: July 5, 2012Inventors: David Allen Burns, Grregory Edward Neal
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Publication number: 20120149692Abstract: The invention is directed to novel crystalline forms of meloxicam. These novel crystalline forms of meloxicam have improved bioavailability, an enhanced rate of dissolution and shorter time to Cmax in blood, as compared to pure meloxicam.Type: ApplicationFiled: February 17, 2012Publication date: June 14, 2012Applicant: THAR PHARMACEUTICALSInventors: Mazen Hanna, Ning Shan, Miranda L. Cheney, David R. Weyna
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Publication number: 20120129845Abstract: This application discloses 5-phenyl-1H-pyridin-2-one and 6-phenyl-2H-pyridazin-3-one derivatives according to generic Formulae I-IV: wherein, variables R, X, Y1, Y2, Y2?, Y3, Y4, n and m are defined as described herein, which inhibit Btk. The compounds disclosed herein are useful to modulate the activity of Btk and treat diseases associated with excessive Btk activity. The compounds are further useful to treat inflammatory and auto immune diseases associated with aberrant B-cell proliferation such as rheumatoid arthritis. Also disclosed are compositions comprising compounds of Formulae I-IV and at least one carrier, diluent or excipient.Type: ApplicationFiled: January 26, 2012Publication date: May 24, 2012Inventors: Nolan James Dewdney, Rama K. Kondru, Bradley E. Loe, Yan Lou, Joel McIntosh, Timothy D. Owens, Michael Soth
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Patent number: 8124603Abstract: The invention is directed to novel crystalline forms of meloxicam. These novel crystalline forms of meloxicam have improved bioavailability, an enhanced rate of dissolution and shorter time to Cmax in blood, as compared to pure meloxicam.Type: GrantFiled: January 22, 2009Date of Patent: February 28, 2012Assignee: Thar PharmaceuticalsInventors: Mazen Hanna, Ning Shan, Miranda L. Cheney, David R. Weyna
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Publication number: 20120035162Abstract: The invention provides a process for the preparation of high purity meloxicam of the Formula (II). The meloxicam raw product is reacted with the solution of potassium hydroxide or potassium carbonate, whereby high purity meloxicam potassium salt monohydrate is produced. Said salt is subsequently treated with mineral or organic acid to yield high-purity meloxicam.Type: ApplicationFiled: October 12, 2011Publication date: February 9, 2012Inventors: Tibor MEZEI, Gyula Simig, Enikó Molnár, Gyula Lukács, Márta Porcs-Makkay, Balázs Volk, Valéria Hofmanné Fekete, Kálmán Nagy, Norbert Mesterházy, György Krasznai, Györgyi Vereczkeyné Donáth, Gyuláné Körtvélyessy, Éva Pécsi
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Patent number: 8097616Abstract: The invention provides a process for the preparation of high purity meloxicam of the Formula (II). The meloxicam raw product is reacted with the solution of potassium hydroxide or potassium carbonate, whereby high purity meloxicam potassium sait monohydrate is produced. Said sait is subsequently treated with mineral or organic acid to yield high-purity meloxicam.Type: GrantFiled: December 16, 2005Date of Patent: January 17, 2012Assignee: Egis Gyogyszergyar Nyilvanosan Mukodo ReszvenytarsasagInventors: Tibor Mezei, Gyula Simig, Enikó Molnár, Gyula Lukács, Márta Porcs-Makkay, Balázs Volk, Valéria Hofmanné Fekete, Kálmán Nagy, Norbert Mesterházy, György Krasznai, Györgyi Vereczkeyné Donáth, Gyuláné Körtvélyessy, Éva Pécsi
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Publication number: 20110319326Abstract: The object of the present invention is benzothiazine derivatives having the capability of inhibiting 11?-HSD1 not only at an enzymatic level but also at a cell level. The compounds of the present invention are of general formula (I). Wherein notably R1 represents a hydrogen or OR1 represents an ester or an ether. R2 represents a naphthyl or a 1, 2, 3, 4-tetrahydro-naphthalene or a biphenyl or phenyl pyridine or a substituted phenyl. R3 represents a methyl or ethyl; R4 and R?4 represent a hydrogen.Type: ApplicationFiled: March 2, 2010Publication date: December 29, 2011Applicant: PIERRE FABRE MEDICAMENTInventors: Michel Perez, Marie Lamothe, Didier Junquero, Yves Rival
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Publication number: 20110262361Abstract: The present invention allows a screening method for identifying novel drugs for the treatment of tuberculosis as well as a diagnostic method for identifying clinical strains that are resistant to these novel drugs. In particular, the present invention relates to a method for screening in vitro drug candidates for the treatment of tuberculosis by interfering with the arabinogalactan biosynthesis, the said method comprising a step of putting into contact a Mycobacterium tuberculosis cell culture overexpressing a protein that performs the transformation of decaprenyl-P-ribose to decaprenyl-P-arabinose and that can be encoded by rv3790 gene or homologues thereof or any open-reading artificial frame whose gene product is identical or homologue to Rv3790 protein, with a drug candidate and then evaluating the percentage of inhibition caused by the drug candidate against a control in an assay test, such as an antibacterial test or an enzymatic test.Type: ApplicationFiled: February 13, 2008Publication date: October 27, 2011Inventors: Giovanna Riccardi, Giulia Manina, Maria Rosalia Pasca
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Publication number: 20110218191Abstract: The invention is directed to a formulation containing NSAIDs or a pharmacologically acceptable salt thereof of and one or more vehicles for the treatment of kidney diseases in cats. Serum creatinine concentrations increase less over time following treatment with NSAID compared to untreated cats.Type: ApplicationFiled: February 28, 2011Publication date: September 8, 2011Applicant: BOEHRINGER INGELHEIM VETMEDICA GMBHInventor: Laura JOHNSTON
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Publication number: 20110212948Abstract: A method of administering meloxicam containing compositions to neonate foals of 6 weeks of age or less is provided. The inventors have discovered that foals of 6 weeks of age or less can have meloxicam administered at a dosage of 0.6 mg/kg without any negative or adverse reaction by the foal. The method also provides a dosing regimen for obtaining first peak plasma concentrations of approximately 800 ng/ml, average plasma concentration levels of 200 ng/ml for 6 hours after a single dose, and sustained plasma concentration levels of 100 ng/ml with twice daily dosing.Type: ApplicationFiled: July 10, 2009Publication date: September 1, 2011Inventors: Giuseppe Pippia, Sharanne Raidal
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Patent number: 8008480Abstract: A process for purifying meloxicam form I from a crude meloxicam, which comprises: i. contacting the crude meloxicam with an amine in a non-aqueous solvent to form a meloxicam salt; ii. isolating the meloxicam salt; iii. dissolving the meloxicam salt in an aqueous solvent to form a salt solution; and iv. adding an acid to the salt solution to precipitate free meloxicam.Type: GrantFiled: March 2, 2009Date of Patent: August 30, 2011Assignee: Norbrook Laboratories LtdInventors: Liam McElroy, Lillian Cromie, Mark Garret
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Publication number: 20110150873Abstract: The invention relates to the use of Broad-Spectrum Chemokine Inhibitors (BSCIs), and in particular members of the acylaminolactam class of pharmaceutical agents, for the prevention, prophylaxis, treatment or amelioration of symptoms of inflammatory diseases. In particular, improved compositions consisting of BSCI agents combined with one or more additional active pharmaceutical agents in order to achieve improved anti-inflammatory efficacy with a reduced side-effect profile are described and claimed.Type: ApplicationFiled: December 10, 2008Publication date: June 23, 2011Applicant: CAMBRIDGE ENTERPRISE LIMITEDInventor: David John Grainger
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Publication number: 20110105479Abstract: This application discloses 5-phenyl-1H-pyridin-2-one and 6-phenyl-2H-pyridazin-3-one derivatives according to generic Formulae I-IV: wherein, variables R, X, Y1, Y2, Y2?, Y3, Y4, n and m are defined as described herein, which inhibit Btk. The compounds disclosed herein are useful to modulate the activity of Btk and treat diseases associated with excessive Btk activity. The compounds are further useful to treat inflammatory and auto immune diseases associated with aberrant B-cell proliferation such as rheumatoid arthritis. Also disclosed are compositions comprising compounds of Formulae I-IV and at least one carrier, diluent or excipient.Type: ApplicationFiled: January 10, 2011Publication date: May 5, 2011Inventors: Nolan James Dewdney, Rama K. Kondru, Bradley E. Loe, Yan Lou, Joel McIntosh, Timothy D. Owens, Michael Soth
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Publication number: 20110046113Abstract: It is intended to provide novel amine compounds which are efficacious against diseases such as infection with HIV virus, rheumatism and cancer metastasis. Namely, amine compounds represented by the following general formula (1): In a typical case, A1 and A2 represent each an optionally substituted monocyclic or polycyclic aromatic heterocycle; W represents cyclic C3-10 alkylene, an optionally substituted monocyclic or polycyclic aromatic heterocycle, a monocyclic or polycyclic aromatic ring or a partly saturated polycyclic aromatic ring; X represents O, CH2, C(?O) or NR11; and D is a group represented by the following general formula (4) or (6). In the formula (6), Q represents a single bond, S, O or NR12; and Y is a group represented by the following general formula (7). —(CR18R19)m3— Or —(CR20R21)m4-z-(CR22R23)m5??(7) z represents an optionally substituted monocyclic or polycyclic aromatic ring. In the formula (6), B represents NR25R26.Type: ApplicationFiled: October 12, 2010Publication date: February 24, 2011Applicant: KUREHA CORPORATIONInventors: Toru YAMAZAKI, Shigeyuki KIKUMOTO, Masahiro ONO, Atsushi SAITOU, Haruka TAKAHASHI, Sei KUMAKURA, Kunitaka HIROSE, Mikiro YANAKA, Yoshiyuki TAKEMURA, Shigeru SUZUKI, Ryo MATSUI
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Patent number: 7879843Abstract: A medicine which contains as an active ingredient a benzothiazin-3-one-compound represented by the formula (1): (wherein n is 3 or 4; R represents ethyl or hydrogen; and R1 represents hologeno, alkoxy, haloalkyl, or haloalkoxy) or a pharmaceutically acceptable salt thereof. It is useful as a therapeutic or preventive agent for arthrosis deformans, chondrodegenerative discases such as chronic articular rheumatism, cancers, gingivitis, etc. Also provided are an intermediate for the compound and a process for producing the compound.Type: GrantFiled: August 26, 2009Date of Patent: February 1, 2011Assignee: Dainippon Sumitomo Pharma Co., Ltd.Inventors: Fumio Samizo, Yoshihiro Horiuchi, Nobuhisa Fukuda, Katsunori Tsuboi, Atsushi Makita
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Publication number: 20100297252Abstract: The present invention is directed to nanoparticulate compositions comprising meloxicam particles having an effective average particle size of less than about 2000 nm.Type: ApplicationFiled: May 26, 2010Publication date: November 25, 2010Inventors: Eugene R. Cooper, Tuula Ryde, John Pruitt, Laura Kline
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Patent number: 7790726Abstract: Compounds are provided that act as potent antagonists of the CCR1 receptor, and have in vivo anti-inflammatory activity. The compounds are generally monocyclic and bicyclic compounds and are useful in pharmaceutical compositions, methods for the treatment of CCR1-mediated diseases, and as controls in assays for the identification of competitive CCR1 antagonists.Type: GrantFiled: August 14, 2006Date of Patent: September 7, 2010Assignee: Chemocentryx, Inc.Inventors: Penglie Zhang, Andrew M. K. Pennell, John J. Kim Wright, Lianfa Li, Edward J. Sullivan, Wei Chen, Kevin Lloyd Greenman
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Patent number: 7759339Abstract: Compounds, pharmaceutical compositions, kits and methods are provided for use with hydroxysteroid dehydrogenases that comprise a compound selected from the group consisting of: wherein the variables are as defined herein.Type: GrantFiled: March 28, 2006Date of Patent: July 20, 2010Assignee: Takeda San Diego, Inc.Inventors: Kathleen Aertgeerts, Nancy K. Brennan, Sheldon X. Cao, Edcon Chang, Andre A. Kiryanov, Yan Liu
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Publication number: 20100129366Abstract: The present invention relates to new thiazole inhibitors of cyclooxygenase, pharmaceutical compositions thereof, and methods of use thereof.Type: ApplicationFiled: November 19, 2009Publication date: May 27, 2010Applicant: AUSPEX PHARMACEUTICALS, INC.Inventors: Thomas G. Gant, Manouchehr Shahbaz
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Publication number: 20100081652Abstract: Disclosed is an extracellular matrix genetranscription inhibitor composition or the like characterized by containing a cinnamoyl compound represented by the formula (I) below: and an inert carrier.Type: ApplicationFiled: March 2, 2006Publication date: April 1, 2010Inventors: Hiroaki Shiraki, Kiyoshi Higashi, Yoshitaka Tomigahara, Junya Takahashi
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Patent number: 7671197Abstract: The present invention relates to a process for the purification of meloxicam and in particular of the impurity composed of 4-hydroxy-2-methyl-N-ethyl-N?-(5-methyl-2-thiazolyl)-2H-1,2-benzothiazine-3-carboxamide-1,1-dioxide and to meloxicam containing a quantity of less than 0.05% of the above-mentioned impurity (“ethylamide”).Type: GrantFiled: October 11, 2005Date of Patent: March 2, 2010Assignee: A.M.S.A. Anonima Materie Sintetiche E Affini S.p.A.Inventors: Enrico Vigano', Ernesto Landonio
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Publication number: 20100016285Abstract: The blow-described formula (I) [Ch.Type: ApplicationFiled: July 23, 2009Publication date: January 21, 2010Applicant: MOCHIDA PHARMACEUTICAL CO., LTD.Inventors: Hideharu UCHIDA, Shinichi OGAWA, Muneyoshi MAKABE, Yoshitaka MAEDA
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Publication number: 20090258856Abstract: The present invention relates to substituted imidazo-pyridinones and imidazo-pyridazinones of general formula wherein Y and R1 to R4 are defined as in claim 1, the tautomers, enantiomers, diastereomers, the mixtures thereof and the salts thereof, which have valuable pharmacological properties, particularly an inhibiting effect on the activity of the enzyme dipeptidylpeptidase-IV (DPP-IV).Type: ApplicationFiled: June 23, 2009Publication date: October 15, 2009Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Matthias ECKHARDT, Norbert HAUEL, Elke LANGKOPF, Frank HIMMELSBACH, Iris KAUFFMANN-HEFNER, Mohammad TADAYYON, Michael MARK
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Patent number: 7598240Abstract: A medicine which contains as an active ingredient a benzothiazin-3-one-compound represented by the formula (1): (wherein n is 3 or 4; R represents ethyl or hydrogen; and R1 represents hologeno, alkoxy, haloalkyl, or haloalkoxy) or a pharmaceutically acceptable salt thereof. It is useful as a therapeutic or preventive agent for arthrosis deformans, chondrodegenerative discases such as chronic articular rheumatism, cancers, gingivitis, etc. Also provided are an intermediate for the compound and a process for producing the compound.Type: GrantFiled: February 28, 2005Date of Patent: October 6, 2009Assignee: Dainippon Sumitomo Pharma Co., Ltd.Inventors: Fumio Samizo, Yoshihiro Horiuchi, Nobuhisa Fukuda, Katsunori Tsuboi, Atsushi Makita
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Patent number: 7595343Abstract: The invention relates to the inhibition of histone deacetylase. The invention provides compounds and methods for inhibiting histone deacetylase enzymatic activity. The invention also provides compositions and methods for treating cell proliferative diseases and conditions.Type: GrantFiled: September 12, 2002Date of Patent: September 29, 2009Assignee: MethylGene, Inc.Inventors: Daniel Delorme, Soon Hyung Woo, Arkadii Vaisburg, Oscar Moradei, Silvana Leit, Stephane Raeppel, Sylvie Frechette, Giliane Bouchain
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Publication number: 20090215757Abstract: The invention provides a process for the preparation of high purity meloxicam of the Formula (II). The meloxicam raw product is reacted with the solution of potassium hydroxide or potassium carbonate, whereby high purity meloxicam potassium salt monohydrate is produced. Said salt is subsequently treated with mineral or organic acid to yield high-purity meloxicam.Type: ApplicationFiled: December 16, 2005Publication date: August 27, 2009Inventors: Tibor Mezei, Gyula Simig, Enikó Molnár, Gyula Lukács, Márta Porcs-Makkay, Balázs Volk, Valéria Hofmanné Fekete, Kálmán Nagy, Norbert Mesterházy, György Krasznai, Györgyi Vereczkeyné Donáth, Gyuláné Körtvélyessy, Éva Pécsi
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Publication number: 20090203680Abstract: The invention is directed to novel crystalline forms of meloxicam. These novel crystalline forms of meloxicam have improved bioavailability, an enhanced rate of dissolution and shorter time to Cmax in blood, as compared to pure meloxicam.Type: ApplicationFiled: January 22, 2009Publication date: August 13, 2009Applicant: Thar PharmaceuticalsInventors: Mazen Hanna, Ning Shan, Miranda L. Cheney, David R. Weyna
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Patent number: 7566707Abstract: The present invention relates to substituted imidazo-pyridinones and imidazo-pyridazinones of general formula wherein Y and R1 to R4 are defined as in claim 1, the tautomers, enantiomers, diastereomers, the mixtures thereof and the salts thereof, which have valuable pharmacological properties, particularly an inhibiting effect on the activity of the enzyme dipeptidylpeptidase-IV (DPP-IV).Type: GrantFiled: June 10, 2004Date of Patent: July 28, 2009Assignee: Boehringer Ingelheim International GmbHInventors: Matthias Eckhardt, Norbert Hauel, Elke Langkopf, Frank Himmelsbach, Iris Kauffmann-Hefner, Mohammad Tadayyon, Michael Mark
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Publication number: 20090163707Abstract: A process for purifying meloxicam form I from a crude meloxicam, which comprises: i. contacting the crude meloxicam with an amine in a non-aqueous solvent to form a meloxicam salt; ii. isolating the meloxicam salt; iii. dissolving the meloxicam salt in an aqueous solvent to form a salt solution; and iv. adding an acid to the salt solution to precipitate free meloxicam.Type: ApplicationFiled: March 2, 2009Publication date: June 25, 2009Inventors: Liam McElroy, Lillian Cromie, Mark Garret
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Publication number: 20090143368Abstract: A composition for inhibiting the extracellular matrix gene transcription comprising a cinnamoyl compound represented by the formula (I): and an inert carrier, or the like.Type: ApplicationFiled: March 2, 2006Publication date: June 4, 2009Inventors: Hiroaki Shiraki, Kiyoshi Higashi, Yoshitaka Tomigahara, Junya Takahashi
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Publication number: 20090099159Abstract: A method of treating or preventing of a disease or condition associated with an increased level of isoforms of amyloid ? peptides (A?) and/or with a changed ratio of levels of A? isoforms and/or with the formation of plaques containing amyloid ? peptide (A?) isoforms in a mammal comprising administering to said mammal an therapeutically effective amount of a compound selected from the formulas Ia, Ib wherein V, W, Y, R2, R3, R5, R6, L1 and i are defined as in claim 1.Type: ApplicationFiled: December 17, 2008Publication date: April 16, 2009Applicants: BOEHRINGER INGELHEIM INTERNATIONAL GMBH, BOEHRINGER INGELHEIM PHARMACEUTICALS, INC.Inventors: Klaus BORNEMANN, Guenter TRUMMLITZ, Bernd BECK, Frank SAMS-DODD, Dagmar KUGLER, Klaus KLINDER, Cornelia DORNER-CIOSSEK, Marcus KOSTKA
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Publication number: 20090048224Abstract: Selected compounds are effective for treatment of pain and diseases, such as inflammation mediated diseases. The invention encompasses novel compounds, analogs, prodrugs and pharmaceutically acceptable derivatives thereof, pharmaceutical compositions and methods for prophylaxis and treatment of diseases and other maladies or conditions involving pain, inflammation, and the like. The subject invention also relates to processes for making such compounds as well as to intermediates useful in such processes.Type: ApplicationFiled: September 5, 2008Publication date: February 19, 2009Applicants: Amgen, Inc., Array BioPharma, Inc.Inventors: Robert D. Groneberg, Benny C. Askew, JR., Derin C. D'Amico, James Zhan, Andras Toro, Youngboo Kim, David A. Mareska, Nianhe Han, Christopher H. Fotsch, Qingyian Liu, Babak Riahi, Kevin Yang, Aiwen Li, Chester Chenguang Yuan, Kaustav Biswas, Scott Harried, Thomas Nguyen, Wenyuan Qian, Jian Jeffrey Chen, Rana Nomak
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Patent number: 7482337Abstract: Disclosed are substituted xanthines of general formula wherein R1 to R4 are defined hereinbelow, the tautomers, the stereoisomers, the mixtures thereof, the prodrugs thereof and the salts thereof, which have valuable pharmacological properties, particularly an inhibitory effect on the activity of the enzyme dipeptidylpeptidase-IV (DPP-IV).Type: GrantFiled: October 28, 2003Date of Patent: January 27, 2009Assignee: Boehringer Ingelheim Pharma GmbH & Co. KGInventors: Frank Himmelsbach, Elke Langkopf, Matthias Eckhardt, Roland Maier, Michael Mark, Mohammad Tadayyon, Ralf R. H. Lotz
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Publication number: 20090017003Abstract: The present invention relates to novel thiosulfonates derivatives. The present invention also provides methods for preventing, treating and/or reducing inflammation-associated diseases in the cardiovascular, connective tissue, pulmonary, gastrointestinal, respiratory, urogenital, nervous or cutaneous systems as well as infective and tumoral diseases employing said compounds.Type: ApplicationFiled: March 1, 2007Publication date: January 15, 2009Applicant: SULFIDRIS S.R.L.Inventors: Piero Del Soldato, Giancarlo Santus, Anna Sparatore
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Patent number: 7419542Abstract: The invention is directed to a method or use of 2,9-dichloro-quinacridone as an alpha crystal phase inhibitor and optionally, 4,11-dichloroquinacridone during the beta-quinacridone or gamma-quinacridone crude pigment particle size reduction processes. The invention is also directed to solid solutions of quinacridone comprising about 98 to about 80 weight % gamma or beta-quinacridone, about 0.1 to about 10 weight % 2,9-dichloroquinacridone and about 0.1 to about 10 weight % 4,11-dichloroquinacridone.Type: GrantFiled: July 18, 2006Date of Patent: September 2, 2008Assignee: Ciba Specialty Chemicals CorporationInventors: Yingxia He, Colin Dennis Campbell, Gordian Schilling, Rhonda Carter, Melissa Wagner, James Thomas Will, Kevin Rodney Gerzevske
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Publication number: 20080188467Abstract: The present disclosure relates to compounds, which are useful for regulating the expression of apolipoprotein A-I (ApoA-I), and their use for treatment and prevention of cardiovascular disease and related disease states, including cholesterol- or lipid-related disorders, such as, for example, atherosclerosis.Type: ApplicationFiled: February 1, 2007Publication date: August 7, 2008Inventors: Norman C.W. Wong, Joseph E.L. Tucker, Henrik C. Hansen, Fabrizio S. Chiacchia, David McCaffrey
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Patent number: 7407950Abstract: The invention concerns compounds of general formula (I), wherein n, X1, X2, X3, X4, Z1, Z2, Z3, Z4, Z5 and W are as defined herein. Said compounds are ligands of the TRPV1 vanilloid receptor, and are therefore, useful for treating diseases associated with TRPV1 receptors, such as pain and inflammation.Type: GrantFiled: June 20, 2007Date of Patent: August 5, 2008Assignee: Sanofi-AventisInventors: Laurent Dubois, Yannick Evanno, Andre Malanda
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Publication number: 20080171737Abstract: The present invention is directed to cyclic sulfonamide derivatives of formula I: or a pharmaceutically acceptable salt thereof, which are monoamine reuptake inhibitors, compositions containing these derivatives, and methods of their use for the prevention and treatment of conditions, including, inter alia, vasomotor symptoms, sexual dysfunction, gastrointestinal disorders and genitourinary disorder, depression disorders, endogenous behaviorial disorder, cognitive disorder, diabetic neuropathy, pain, and other diseases or disorders.Type: ApplicationFiled: December 12, 2007Publication date: July 17, 2008Applicant: WyethInventors: Andrew Fensome, Joel Adam Goldberg, Casey Cameron McComas, Charles William Mann, Edward George Melenski, Joseph Peter Sabatucci, Richard Page Woodworth