The Six-membered Hetero Rings Are Bonded Directly To Each Other Patents (Class 514/334)
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Publication number: 20140155401Abstract: The present invention relates to novel substituted 2,4?- and 3,4?-bipyridine derivatives, to processes for their preparation, to their use for the treatment and/or prophylaxis of diseases and to their use for preparing medicaments for the treatment and/or prophylaxis of diseases, preferably for the treatment and/or prevention of hypertension and other cardiovascular disorders.Type: ApplicationFiled: February 7, 2014Publication date: June 5, 2014Applicant: BAYER INTELLECTUAL PROPERTY GMBHInventors: Peter NELL, Walter Hübsch, Barbara ALBRECHT-KÜPPER, Jörg KELDENICH, Andreas KNORR
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Publication number: 20140148438Abstract: There is provided compositions and methods for the treatment of respiratory conditions such as pulmonary hypertension and sickle-cell disease in a patient in need thereof. The composition and method are for treating a patient in need thereof by inhalation of a composition containing amino acid ester compounds comprising at least one nitric oxide releasing group and pharmaceutical salts thereof.Type: ApplicationFiled: September 22, 2011Publication date: May 29, 2014Inventor: Michael Farber
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Publication number: 20140135328Abstract: The present invention relates to compounds of the formula I, wherein A, D, E, L, G, R10, R30, R40, R50 and R60 have the meanings indicated in the claims, which are valuable pharmaceutical active compounds. They are inhibitors of the protease cathepsin A, and are useful for the treatment of diseases such as atherosclerosis, heart failure, renal diseases, liver diseases or inflammatory diseases, for example. The invention furthermore relates to processes for the preparation of the compounds of the formula I, their use and pharmaceutical compositions comprising them.Type: ApplicationFiled: January 17, 2014Publication date: May 15, 2014Applicant: SANOFIInventors: Sven Ruf, Thorsten Sadowski, Klaus Wirth, Herman Schreuder, Christian Buning
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Publication number: 20140135329Abstract: The present invention provides pyridine and pyrazine derivatives which restore or enhance the function of mutant and/or wild type CFTR to treat cystic fibrosis, primary ciliary dyskinesia, chronic bronchitis, chronic obstructive pulmonary disease, asthma, respiratory tract infections, lung carcinoma, xerostomia and keratoconjunctivitis sire, or constipation (IBS, IBD, opioid induced). Pharmaceutical compositions comprising such derivatives are also encompassed.Type: ApplicationFiled: June 20, 2013Publication date: May 15, 2014Inventors: Urs BAETTIG, Kamlesh BALA, Emma BUDD, Lee EDWARDS, Catherine HOWSHAM, Glyn Alan HUGHES, Darren Mark LEGRAND, Katrin SPIEGEL
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Patent number: 8680118Abstract: A compound of formula: wherein Ar1, Ar2, V, X, R3, R4, and m are as disclosed herein or a pharmaceutically acceptable salt thereof (a “Cyclo(hetero)alkenyl Compound”); compositions comprising an effective amount of a Cyclo(hetero)alkenyl Compound; and methods for treating or preventing, e.g., pain, UI, an ulcer, IBD, or IBS in an animal, comprising administering to an animal in need thereof an effective amount of a Cyclo(hetero)alkenyl Compound are disclosed herein.Type: GrantFiled: June 18, 2012Date of Patent: March 25, 2014Assignee: Purdue Pharma L.P.Inventors: Donald J. Kyle, Qun Sun, Laykea Tafesse
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Patent number: 8673923Abstract: Methods and compositions relating to TIC10 are described according to aspects of the present invention. The compositions and methods have utility in treating disease, particularly cancer in a subject in need thereof, including a human subject as well as subjects of other species. The compositions have utility in treating brain cancer in a subject in need thereof.Type: GrantFiled: April 30, 2012Date of Patent: March 18, 2014Assignee: The Penn State Research FoundationInventors: Wafik S. El-Deiry, Joshua E. Allen, Gen Sheng Wu
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Publication number: 20140072536Abstract: Disclosed herein are ?7?1 integrin modulatory agents and methods of using such to treat conditions associated with decreased ?7?1 integrin expression or activity, including muscular dystrophy. In one example, methods for treating a subject with muscular dystrophy are disclosed. The methods include administering an effective amount of an ?7?1 integrin modulatory agent to the subject with muscular dystrophy, wherein the ?7?1 integrin modulatory agent increases ?7?1 integrin expression or activity as compared to ?7?1 integrin expression or activity prior to treatment, thereby treating the subject with muscular dystrophy. Also disclosed are methods of enhancing muscle regeneration, repair, or maintenance in a subject and methods of enhancing ?7?1 integrin expression by use of the disclosed ?7?1 integrin modulatory agents. Methods of prospectively preventing or reducing muscle injury or damage in a subject are also disclosed.Type: ApplicationFiled: March 15, 2013Publication date: March 13, 2014Applicant: Board of Regents of the Nevada System of Higher Education On Behalf of the University of NevadaInventors: Ryan Wuebbles, Dean Burkin
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Publication number: 20140057916Abstract: This invention relates to substituted 4-pyridones of formula 1 and their use as inhibitors of neutrophil elastase activity, pharmaceutical compositions containing the same, and methods of using the same as agents for treatment and/or prevention of pulmonary, gastrointestinal and genitourinary diseases, inflammatory diseases of the skin and the eye and other auto-immune and allergic disorders, allograft rejection, and oncological diseases.Type: ApplicationFiled: August 20, 2013Publication date: February 27, 2014Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Thorsten OOST, Dennnis FIEGEN, Christian GNAMM, Sandra HANDSCHUH, Stefan PETERS, Gerald Juergen ROTH
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Publication number: 20140057949Abstract: This disclosure provides beverage products comprising a compound of Formula I, such as anatabine, suitable for human consumption.Type: ApplicationFiled: October 31, 2013Publication date: February 27, 2014Applicant: Rock Creek Pharmaceuticals, Inc.Inventor: Jonnie R. Williams
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Publication number: 20140057892Abstract: The present disclosure relates to HIF-1? prolyl hydroxylase inhibitors, compositions which comprise the HIF-1? prolyl hydroxylase inhibitors described herein and to methods for controlling, inter alia, Peripheral Vascular Disease (PVD), Coronary Artery Disease (CAD) heart failure, ischemia, and anemia.Type: ApplicationFiled: November 4, 2013Publication date: February 27, 2014Applicant: Akebia Therapeutics, Inc.Inventors: Richard Masaru Kawamoto, Shengde Wu, Artem G. Evdokimov, Kenneth D. Greis, Angelique Sun Boyer, Namal C. Warshakoon
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Patent number: 8653109Abstract: The present invention relates to novel substituted 2,4?- and 3,4?-bipyridine derivatives, to processes for their preparation, to their use for the treatment and/or prophylaxis of diseases and to their use for preparing medicaments for the treatment and/or prophylaxis of diseases, preferably for the treatment and/or prevention of hypertension and other cardiovascular disorders.Type: GrantFiled: August 30, 2007Date of Patent: February 18, 2014Assignee: Bayer Intellectual Property GmbHInventors: Peter Nell, Walter Hübsch, Barbara Albrecht-Küpper, Joerg Keldenich, Andreas Knorr
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Patent number: 8653276Abstract: The present invention is directed to compounds of the general formula: as defined herein, and pharmaceutical compositions thereof. The invention is also directed to their therapeutic use as urotensin II receptor antagonists, e.g., in the treatment of cardiac, coronary, and central nervous system disorders. In particular embodiments, the invention relates to 5,6-bisaryl-2-pyridinecarboxamides, to their preparation and to their therapeutic use as urotensin II receptor antagonists.Type: GrantFiled: May 15, 2013Date of Patent: February 18, 2014Assignee: SANOFIInventors: Jean-Michel Altenburger, Valerie Fossey, Daniel Galtier, Frederic Petit
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Publication number: 20140045873Abstract: The present invention provides compounds of formula (I) wherein A1, A2, R1, D1, D2, Y3 and X are as defined in the claims. The invention further relates to compositions which comprise these compounds and to their use in agriculture or horticulture for controlling or preventing infestation of plants by phytopathogenic microorganisms, preferably fungi.Type: ApplicationFiled: November 10, 2011Publication date: February 13, 2014Applicant: SYNGENTA PARTICIPATIONS AGInventors: Stephan Trah, Werner Zambach, Daniel Stierli, Kurt Nebel, Andrea Bortolato
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Publication number: 20140037547Abstract: The present invention relates to cGMP protein kinase (PKG) and regulatory domains and methods of use thereof. The structural determination of PKG domains is also described. cGMP independent PKG activators and uses thereof are also described.Type: ApplicationFiled: March 13, 2013Publication date: February 6, 2014Applicant: The University of Vermont and State Agricultural CollegeInventors: Wolfgang Dostmann, Brent W. Osborne, Thomas M. Moon
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Patent number: 8637548Abstract: A compound of formula: where Ar1, Ar2, X, R3, and m are as disclosed herein or a pharmaceutically acceptable salt thereof (a “Cycloheteroalkenyl Compound”); compositions comprising an effective amount of a Cycloheteroalkenyl Compound; and methods for treating or preventing pain, UI, an ulcer, IBD, IBS, an addictive disorder, Parkinson's disease, parkinsonism, anxiety, epilepsy, stroke, a seizure, a pruritic condition, psychosis, a cognitive disorder, a memory deficit, restricted brain function, Huntington's chorea, amyotrophic lateral sclerosis, dementia, retinopathy, a muscle spasm, a migraine, vomiting, dyskinesia, or depression in an animal comprising administering to an animal in need thereof an effective amount of a Cycloheteroalkenyl Compound are disclosed herein.Type: GrantFiled: September 21, 2010Date of Patent: January 28, 2014Assignee: Purdue Pharma L.P.Inventors: Qun Sun, Xin Wen
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Publication number: 20140005195Abstract: The present invention relates to novel bipyridine sulfonamide derivatives of formula (I) and their use for the treatment and/or prophylaxis of a neurodegenerative disease or condition, particularly Alzheimers disease (AD), a cardiovascular disease or a pathology involving ischemia. Additionally, processes for preparing such derivatives5 and pharmaceutical compositions comprising them are provided.Type: ApplicationFiled: November 21, 2011Publication date: January 2, 2014Applicant: Noscira, S.A.Inventors: Francisco Palomo Nicolau, Jorge Sánchez-Quesada, Javier López Ogalla, Félix Hernández Juan, Javier Villasante Prieto, Miguel Medina Padilla, Ana Fuertes Huerta, Juan Manuel Dominguez Correa, Susan Herrero Santos, Mercedes Alonso Cascón
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Publication number: 20140005178Abstract: The present disclosure relates to new azabiphenylaminobenzoic acid derivatives of formula (I); as well as processes for their preparation, pharmaceutical compositions comprising them, and their use in therapy as inhibitors of the dehydroorotate dihydrogenase (DHODH).Type: ApplicationFiled: August 12, 2013Publication date: January 2, 2014Applicant: Almirall, S.A.Inventors: Julio Cesar CASTRO PALOMINO LARIA, Emma Terricabras Belart, Montserrat Erra Sola, Eloisa Navarro Romero, Siliva Fonquerna Pou, Aranzazu Cardus Figueras, Maria Estrella Lozoya Toribio
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Publication number: 20130338163Abstract: The invention relates to compounds that are useful as immunosuppressive agents and for treating and preventing inflammatory conditions, allergic disorders, and immune disorders.Type: ApplicationFiled: September 18, 2012Publication date: December 19, 2013Applicant: Synta Phamaceuticals Corp.Inventor: Shoujun Chen
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Patent number: 8609697Abstract: An aqueous-based composition which includes a) at least one bispyridinium alkane (for example octenidine) and b) at least one stabilizer selected from antioxidants, complexing agents, reducing agents, UV filters and photoprotective agents, in particular ?-tocopherol, and BHT. The composition can also include c) one or more auxiliaries selected from, for example, nonionic surfactants, ethers, solvents and polymers, in particular fatty alcohol alkoxylates and alkoxylated fatty acid monoglycerides. The presence of the stabilizer reduces or prevents the appearance of decomposition products of bispyridinium alkanes and, in the case of the presence of auxiliaries, of decomposition products of the auxiliaries, such as ethers and peroxides.Type: GrantFiled: February 18, 2009Date of Patent: December 17, 2013Assignee: Air Liquide Sante (International)Inventors: Wolfgang Beilfuss, Andreas Dettmann, Sabine Behrends, Mona Golombiewski, Thomas Spuida, Elke Kassens
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Publication number: 20130324530Abstract: The present invention provides a compound of formula (I): and pharmaceutically acceptable salts, enantiomers, stereoisomers, rotamers, tautomers, diastereomers, or racemates thereof. Also provided are pharmaceutical compositions containing these compounds and methods of treating a disease or condition mediated by CDK9 using these compounds and compositions.Type: ApplicationFiled: November 17, 2011Publication date: December 5, 2013Inventors: William R. Antonios-McCrea, Paul A. Barsanti, Cheng Hu, Xianming Jin, Eric J. Martin, Yue Pan, Keith B. Pfister, Martin Sendzik, James Sutton, Lifeng Wan
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Patent number: 8592458Abstract: The invention relates to the design and synthesis of 3-arylidene-anabaseine compounds that exhibit enhanced selectivity toward alpha7 nicotinic receptors. The compounds are expected to be useful in treating a wide variety of conditions, including neurodegenerative conditions such as Alzheimer's Disease, neurodevelopmental diseases such as schizophrenia, and certain peripherally located inflammations mediated by macrophage infiltration.Type: GrantFiled: December 16, 2011Date of Patent: November 26, 2013Assignee: University of Florida Research Foundation, Inc.Inventors: William Reade Kem, Ferenc Soti
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Publication number: 20130310375Abstract: The present invention relates to compositions and methods for modulating the Wnt signaling pathway.Type: ApplicationFiled: July 22, 2013Publication date: November 21, 2013Applicant: IRM LLCInventors: Dai Cheng, Guobao Zhang, Dong Han, Wenqi Gao, Shifeng Pan
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Publication number: 20130303507Abstract: The present invention provides a compound of formula (II): where R1 is a substituted alkyl, heterocyclic, or cycloalkyl, group, and pharmaceutically acceptable salts, enantiomers, stereoisomers, rotamers, tautomers, diastereomers, or racemates thereof, and pharmaceutical compositions comprising these compounds. Also provided are methods of using these compounds to treat a disease or condition mediated by CDK9, such as cancers and other conditions described herein.Type: ApplicationFiled: January 20, 2012Publication date: November 14, 2013Applicant: Novartis AGInventors: William R. Antonios-McCrea, Paul A. Barsanti, Cheng Hu, Xianming Jin, Eric Martin, Yue Pan, Xiaodong Lin, Keith B. Pfister, Paul A. Renhowe, Martin Sendzik, James Sutton, Lifeng Wan
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Patent number: 8580738Abstract: The present invention discloses methods to prevent and treat cardiovascular disorders, hi certain aspects the methods are drawn to releasing endogenous calcitonin-gene related peptide from intrinsic cardiac adrenergic cells within the heart. In further aspects, a combination of a ?2 adrenergic receptor agonist (?2-AR agonist) and a vasodilator can be used in treating reperfusion injury.Type: GrantFiled: April 30, 2008Date of Patent: November 12, 2013Assignee: The Board of Regents of the University of Texas SystemInventors: Ming-He Huang, Yochai Birnbaum, Barry F. Uretsky
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Patent number: 8575199Abstract: The invention relates to compounds of formula IA? and pharmaceutically acceptable derivatives thereof, compositions comprising an effective amount of a compound of formula IA? or a pharmaceutically acceptable derivative thereof, and methods for treating or preventing a condition such as pain, UI, an ulcer, IBD and IBS, comprising administering to an animal in need thereof an effective amount of a compound of formula IA? or a pharmaceutically acceptable derivative thereof.Type: GrantFiled: February 14, 2012Date of Patent: November 5, 2013Assignee: Purdue Pharma L.P.Inventor: Laykea Tafesse
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Publication number: 20130287833Abstract: Medical devices having a catalyst capable of catalyzing the generation of nitric oxide in vivo and methods of treating a vascular condition using the devices are provided.Type: ApplicationFiled: June 21, 2013Publication date: October 31, 2013Inventors: Thierry Glauser, Stephen D. Pacetti, Paul M. Consigny
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Publication number: 20130281428Abstract: Novel compounds or salts thereof, or crystals thereof, which inhibit Axl and are useful for treating diseases caused by Axl hyperfunction, diseases associated with Axl hyperfunction and/or diseases accompanied by Axl hyperfunction are provided. Pyridone derivatives represented by the formula (1) having various substituents or salts thereof, or crystals thereof (where R1, R2, R3, R5, R6, A, W, X and n in the formula (1) are as defined in the specification, respectively) are provided.Type: ApplicationFiled: January 30, 2013Publication date: October 24, 2013Inventors: Hitoshi Ohki, Masahiro Ota, Kosuke Takeuchi, Hideaki Watanabe, Akitake Yamaguchi, Yoshihiro Shibata, Yuichi Tominaga, Takeshi Jimbo, Keijiro Kobayashi, Katsuhiro Kobayashi, Daisuke Fukatsu
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Publication number: 20130274272Abstract: The present disclosure provides methyl/difluorophenyl-methoxy substituted pyridinone-pyridinyl compounds, methyl-pyridinyl-methoxy substituted pyridinone-pyridinyl compounds, and methyl-pyrimidinyl-methoxy substituted pyridinone-pyridinyl compounds useful in the treatment of p38 kinase mediated diseases, such as lymphoma and auto-inflammatory disease, having the structure of Formula (I): wherein R1, R2, R3 and X are as defined in the detailed description; pharmaceutical compositions comprising at least one of the compounds; and methods for treating p38 kinase mediated diseases using the compound.Type: ApplicationFiled: June 7, 2013Publication date: October 17, 2013Inventors: Shaun R. Selness, Joseph B. Monahan, John F. Schindler, Balekudru Devadas, Susan L. Hockerman
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Patent number: 8546396Abstract: The present invention relates to compounds of formulae 1 and 2 and methods for modulating the Wnt signaling pathway using these compounds, wherein A1, A2, B, Y and Z all represent rings.Type: GrantFiled: March 1, 2010Date of Patent: October 1, 2013Assignee: IRM LLCInventors: Dai Cheng, Guobao Zhang, Dong Han, Wenqi Gao, Shifeng Pan
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Publication number: 20130252974Abstract: The present invention relates to 5,6-bisaryl-2-pyridinecarboxamides, to their preparation and to their therapeutic use as urotensin II receptor antagonists.Type: ApplicationFiled: May 15, 2013Publication date: September 26, 2013Applicant: SANOFIInventors: Jean-Michel Altenburger, Valerie Fossey, Daniel Galtier, Frederic Petit
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Patent number: 8541454Abstract: An antimicrobially effective composition includes a) at least 0.15% by weight of bispyridinium alkane, b) at least 3.5% by weight of humectant and c) water. Upon dilution with water, the composition produces a solution with an osmolality of from 230 to 350 mOsmol/kg and is free from surfactant. It is used as an antiseptic and is suitable for use in a method for the disinfection of injured or uninjured skin of a human being or animal, preference being given to use in the case of newborns, in particular those born prematurely.Type: GrantFiled: June 9, 2011Date of Patent: September 24, 2013Assignee: L'Air Liquide, Societe Anonyme pour l'Etude et l'Exploitation des Procedes Georges ClaudeInventors: Sabine Behrends, Andreas Dettmann, Mona Golombiewski, Elke Kassens
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Publication number: 20130225548Abstract: A main object of the present invention is to provide a novel pyridine derivative represented by the following general formula [1] or a pharmaceutically acceptable salt thereof. In formula [1], R represents an aryl group or a heteroaryl group, which may be substituted by an optionally substituted alkyl group, a hydroxy group, a halogen atom or a group represented by general formula [2]. In formula [2], -L1-L2-L3-RA ??[2] L1 and L3 independently represent a single bond, an alkylene group or a cycloalkylene group; L2 represents a single bond, O, or NRB; RB represents H or an optionally substituted alkyl group; and RA represents B, an amino group, a cyano group, a hydroxy group, an alkoxy group, an aryl group, a monoalkylamino group, a dialkylamino group, a carbamoyl group, an alkyloxycarbonyl group, a monoalkylaminocarbonyl group, a dialkylaminocarbonyl group, an alkylcarbonylamino group, and a saturated heterocyclic group, among other groups.Type: ApplicationFiled: October 27, 2011Publication date: August 29, 2013Applicant: NIPPON SHINYAKU CO., LTD.Inventors: Hidetaka Fujihara, Hiroyuki Sugiyama, Takashi Tsuji, Takara Ino, Yoshinari Haruta
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Publication number: 20130225567Abstract: 5-alkynyl-pyridine of general formula (I) their use as SMAC mimetics, pharmaceutical compositions containing them, and their use as a medicaments for the treatment and/or prevention of diseases characterized by excessive or abnormal cell proliferation and associated conditions such as cancer. The groups R1 to R5 have the meanings given in the claims and in the specification.Type: ApplicationFiled: February 19, 2013Publication date: August 29, 2013Applicant: Boehringer Ingelheim International GmbHInventors: Ulrich REISER, Gerd BADER, Walter SPEVAK, Andreas STEFFEN, Alastair L. PARKES
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Publication number: 20130210795Abstract: The present application relates to novel substituted dicyanopyridines, to processes for their preparation, to their use for the treatment and/or prophylaxis of diseases and to their use for preparing medicaments for the treatment and/or prophylaxis of diseases, preferably for the treatment and/or prophylaxis of cardiovascular disorders.Type: ApplicationFiled: June 27, 2011Publication date: August 15, 2013Applicant: BAYER INTELLECTUAL PROPERTY GMBHInventors: Alexandros Vakalopoulos, Daniel Meibom, Peter Nell, Frank Sussmeier, Barbara Albrecht-Kupper, Katja Zimmermann, Joerg Keldenich, Dirk Schneider, Ursula Krenz
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Patent number: 8507531Abstract: Disclosed herein are novel zinc ionophores, zinc chelators and/or zinc complexes with enhanced aqueous solubility. Methods of treating cancer using at least one zinc ionophore and/or zinc chelator are also disclosed. Also disclosed herein are compositions and methods for treating cancer with combination therapy using at least one texaphyrin metal complex and at least one zinc ionophore or the respective pharmaceutically acceptable derivatives or salts thereof.Type: GrantFiled: October 15, 2010Date of Patent: August 13, 2013Inventors: Darren Magda, Jonathan L. Sessler
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Publication number: 20130202573Abstract: Described herein are compounds useful in the modulation of blood uric acid levels, formulations containing them and methods of using them. In some embodiments, the compounds described herein are used in the treatment or prevention of disorders related to aberrant levels of uric acid.Type: ApplicationFiled: June 15, 2011Publication date: August 8, 2013Applicant: Ardea Biosciences, Inc.Inventors: Samedy Ouk, Esmir Gunic, Jean-Michel Vernier, Chixu Chen
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Publication number: 20130197013Abstract: The invention relates to cyclopropylamine compounds, in particular the compounds of Formula (I), and their use in therapy, including e.g. in the treatment or prevention of cancer, a neurological disease or condition, or viral infection.Type: ApplicationFiled: July 27, 2011Publication date: August 1, 2013Inventors: Mathew Colin Thor Fyfe, Alberto Ortega Muñoz, Julio Castro-Palomino Laria, Marc Martinell Pedemonte, Maria de los Ángeles Estiarte-Martínez, Nuria Valls Vidal
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Publication number: 20130195780Abstract: A skin care product includes a compound of Formula I, IA, or IB (e.g., anatabine), or a salt thereof, and a suitable cosmetic or pharmaceutical vehicle. In some aspects, the skin care product is a paste, cream, lotion, gel, moisturizer, cleanser, or sunscreen. In some embodiments, the skin care product is applied topically to reduce inflammation, redness, and/or irritation, and/or to improve the appearance of the skin. In other embodiments, the skin care product is applied topically to treat an autoimmune and/or dermatological condition such as acne, psoriasis, and/or rosacea.Type: ApplicationFiled: March 14, 2013Publication date: August 1, 2013Applicant: ROCK CREEK PHARMACEUTICALS, INC.Inventor: Rock Creek Pharmaceuticals, Inc.
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Publication number: 20130197028Abstract: Agonists and antagonists of nAChR?7 and their use as therapeutic agents for treating and managing inflammatory bowel diseases (IBD), such as Crohn's disease (CD) and ulcerative colitis (UC), are disclosed. Agonists and antagonists of nAChR?7 and their use as therapeutic agents for treating and managing inflammatory bowel diseases (IBD), such as Crohn's disease (CD) and ulcerative colitis (UC), are disclosed.Type: ApplicationFiled: June 24, 2011Publication date: August 1, 2013Applicants: OKLAHOMA MEDICAL RESEARCH FOUNDATION, THE JOHNS HOPKINS UNIVERSITYInventors: Xuhang Li, Philip Alex, Michael B. Centola
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Publication number: 20130196952Abstract: The invention relates to compounds of Formula (1) and to processes for the preparation of intermediates used in the preparation of compositions containing and the uses of such derivatives. The compounds according to the present invention are useful in numerous diseases in which ALK protein is involved or in which inhibition of ALK activity may induce benefit, especially for the treatment of cancer mediated by a mutated EML4-ALK fusion protein.Type: ApplicationFiled: May 4, 2011Publication date: August 1, 2013Applicant: PFIZER INC.Inventors: Mark Edward Bunnage, Andrew Simon Cook, Jingrong Jean Cui, Kevin Nell Dack, Judith Gail Deal, Danlin Gu, Mingying He, Patrick Stephen Johnson, Ted William Johnson, Phuong Thi Quy Le, Cynthia Louise Palmer, Hong Shen
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Publication number: 20130184259Abstract: The present invention relates to compounds useful as inhibitors of protein kinases. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders. The invention also provides processes for preparing the compounds of the invention and intermediate compounds useful in these processes.Type: ApplicationFiled: November 16, 2012Publication date: July 18, 2013Applicant: VERTEX PHARMACEUTICALS INCORPORATEDInventor: VERTEX PHARMACEUTICALS INCORPORATED
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Publication number: 20130172354Abstract: The present invention provides a compound of formula (I): and pharmaceutically acceptable salts, enantiomers, stereoisomers, rotamers, tautomers, diastereomers, or racemates thereof. Also provided is a method of treating a disease or condition mediated by CDK9.Type: ApplicationFiled: February 21, 2013Publication date: July 4, 2013Applicant: NOVARTIS AGInventor: Novartis AG
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Patent number: 8476269Abstract: The present invention provides pyridine and pyrazine derivatives which restore or enhance the function of mutant and/or wild type CFTR to treat cystic fibrosis, primary ciliary dyskinesia, chronic bronchitis, chronic obstructive pulmonary disease, asthma, respiratory tract infections, lung carcinoma, xerostomia and keratoconjunctivitis sire, or constipation (IBS, IBD, opioid induced). Pharmaceutical compositions comprising such derivatives are also encompassed.Type: GrantFiled: July 9, 2012Date of Patent: July 2, 2013Assignee: Novartis AGInventors: Urs Baettig, Kamlesh Jagdis Bala, Emma Budd, Lee Edwards, Catherine Howsham, Glyn Alan Hughes, Darren Mark Legrand, Katrin Spiegel
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Patent number: 8476277Abstract: The invention relates to compounds of formula IA and pharmaceutically acceptable derivatives thereof, compositions comprising an effective amount of a compound of formula IA or a pharmaceutically acceptable derivative thereof, and methods for treating or preventing a condition such as pain, UI, an ulcer, IBD and IBS, comprising administering to an animal in need thereof an effective amount of a compound of formula IA or a pharmaceutically acceptable derivative thereof.Type: GrantFiled: April 25, 2008Date of Patent: July 2, 2013Assignee: Purdue Pharma L.P.Inventor: Laykea Tafesse
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Patent number: 8475850Abstract: Compositions and methods for enhancing heavy metal detoxification are described. The compositions and methods described provide enhanced activity of key detoxification systems including that the induction of phase II detoxification enzymes, such as glutathione S-transferases (GSTs), and NADPH quinone reductase (NQO1) activity.Type: GrantFiled: January 18, 2012Date of Patent: July 2, 2013Assignee: Metaproteomics, LLCInventors: Matthew L. Tripp, Veera Konda, Amy J. Hall, Anu Desai, Jeffrey S. Bland
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Patent number: 8466292Abstract: The present invention is directed to compounds of the general formula: as well as pharmaceutical compositions thereof. The invention is also directed to their therapeutic use as urotensin II receptor antagonists, e.g., in the treatment of cardiac, coronary, and central nervous system disorders. In particular embodiments, the invention relates to 5,6-bisaryl-2-pyridinecarboxamides, to their preparation and to their therapeutic use as urotensin II receptor antagonists.Type: GrantFiled: August 6, 2010Date of Patent: June 18, 2013Assignee: SanofiInventors: Jean-Michel Altenburger, Valérie Fossey, Daniel Galtier, Frédéric Petit
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Publication number: 20130150377Abstract: The invention relates to tetrahydropyridinyl and dihydropyrrolyl compounds of Formula (I): and pharmaceutically acceptable salts, prodrugs, or solvates thereof, wherein X, Y, Z, R1, R2, m, and n are defined as set forth in the specification. The invention is also directed to the use of compounds of Formula (I) to treat a disorder responsive to the blockade of calcium channels, and particularly N-type calcium channels. Compounds of the present invention are especially useful for treating pain.Type: ApplicationFiled: November 13, 2012Publication date: June 13, 2013Applicants: SHIONOGI & CO., LTD., PURDUE PHARMA, L.P.Inventors: PURDUE PHARMA, L.P., SHIONOGI & CO., LTD.
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Publication number: 20130123239Abstract: The invention relates to compounds of Formula I and pharmaceutically acceptable derivatives thereof, compositions comprising an effective amount of a compound of Formula I or a pharmaceutically acceptable derivative thereof, and methods for treating or preventing a condition such as pain, UI, an ulcer, IBD and IBS, comprising administering to an animal in need thereof an effective amount of a compound of Formula I or a pharmaceutically acceptable derivative thereof.Type: ApplicationFiled: June 22, 2011Publication date: May 16, 2013Inventor: Noriyuki Kurose
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Patent number: 8440652Abstract: Compounds for the inhibition of mammalian Ste20-like kinase 1 (MST1) are disclosed, along with compositions comprising them and methods of their use in the treatment, management or prevention of an inflammatory or autoimmune diseases or disorders.Type: GrantFiled: March 2, 2012Date of Patent: May 14, 2013Assignee: Lexicon Pharmaceuticals, Inc.Inventors: David John Augeri, Jeffrey Thomas Bagdanoff, Simon David Peter Baugh, Marianne Carlsen, Kenneth Gordon Carson, John Anthony Gilleran, Wei He, Tamas Oravecz, Konstantin Salojin, Leonard Sung
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Patent number: 8440672Abstract: The instant invention provides compounds of Formula I which are 5-lipoxygenase activating protein inhibitors. Compounds of Formula (I) are useful as anti-atherosclerotic, anti-asthmatic, anti-allergic, anti-inflammatory and cytoprotective agents.Type: GrantFiled: August 29, 2007Date of Patent: May 14, 2013Assignee: Merck Sharp & Dohme Corp.Inventors: Anthony Ogawa, Feroze Ujjainwalla, Ellen K. Vande Bunte, Lin Chu, Debra Ondeyka, Ihor Kopka, Bing Li, Hyun Ok, Minal J. Patel, Jinyou Xu, Rosemary Sisco