Chalcogen Bonded Indirectly To The Five-membered Hetero Ring By Acyclic Nonionic Bonding Patents (Class 514/428)
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Publication number: 20120121724Abstract: The present invention is related to the composition and methods of manufacture of orally-dissolvable, edible films as a vehicle for the non-invasive administration of nitroglycerin, as well as other therapeutic agents either with or without nitroglycerin, through the mucosal tissues of the oral cavity. The films include a water soluble film-forming polymer such as pullulan. Methods for producing the films are also disclosed.Type: ApplicationFiled: January 20, 2012Publication date: May 17, 2012Inventor: Todd Maibach
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Publication number: 20120122951Abstract: The development of a skin-whitening agent which has a lower molecular weight, can be synthesized through a fewer steps and can be produced at low cost has been demanded. Thus, it is provided by the present invention a skin-whitening agent including one or more compounds selected from the group consisting of 4-cis-hydroxyproline and its derivative and/or its salt, a skin-whitening composition for external formulation to the skin, a cosmetic composition and a pharmaceutical composition, each of which contains the skin-whitening agent of the invention, and a cosmetic method for whitening the skin, which includes a step of administering one or more compounds selected from the group consisting of 4-cis-hydroxyproline and its derivative and/or its salt. In the skin-whitening agent and the cosmetic method for whitening the skin of the invention, the 4-cis-hydroxyproline may be 4-cis-L-hydroxyproline and/or 4-cis-D-hydroxyproline.Type: ApplicationFiled: March 4, 2010Publication date: May 17, 2012Inventors: Rikako Suzuki, Yosuke Tojo, Chieko Mizumoto, Kiyotaka Hasegawa, Yutaka Ashida, Jun-ichi Hosoi, Kiyoshi Sato
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Patent number: 8173637Abstract: A pharmaceutical composition that contains an atypical antipsychotic drug and succinic acid, fumaric acid or a mixture of succinic acid and fumaric acid.Type: GrantFiled: September 5, 2008Date of Patent: May 8, 2012Assignee: Handa Pharmaceuticals, LLCInventors: Fang-yu Liu, Zhi-qun Shen
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Patent number: 8173631Abstract: Compounds exhibiting calcium receptor antagonist activity that are safe and orally administrable having Formula (I) or pharmaceutically acceptable salts thereofType: GrantFiled: June 23, 2011Date of Patent: May 8, 2012Assignee: Daiichi Sankyo Company, LimitedInventors: Akira Nakao, Kentoku Gotanda, Kazumasa Aoki, Shimpei Hirano, Yoshiharu Hiruma, Takeshi Shiiki
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Patent number: 8173700Abstract: The present invention relates to salts of substituted allophanates, methods for their production, medicaments containing said compounds and the use of said compound for the production of medicaments.Type: GrantFiled: May 17, 2006Date of Patent: May 8, 2012Assignee: Gruenenthal GmbHInventors: Robert Frank, Ruth Jostock, Hans Schick, Fritz Theil, Olga Groeger, Rene Kudick, Helmut Sonnenschein, Birgitta Henkel
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Patent number: 8168674Abstract: Administration of a loop diuretic in nebulized dry powder form directly to a patient's lungs for treating bronchial disease.Type: GrantFiled: February 21, 2003Date of Patent: May 1, 2012Assignee: Microdose Therapeutx, Inc.Inventor: Andrew Abrams
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Patent number: 8163794Abstract: The invention provides a crystalline hydrochloride salt of (S)-3-[(S)-1-(4-chlorophenoxy)-2-methylpropyl]pyrrolidine. This invention also provides pharmaceutical compositions comprising the crystalline salt, processes and intermediates for preparing the crystalline salt, and methods of using the crystalline salt to treat diseases.Type: GrantFiled: June 30, 2011Date of Patent: April 24, 2012Assignee: Theravance, Inc.Inventors: Daisuke Roland Saito, Miroslav Rapta
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Publication number: 20120095004Abstract: The invention relates to substituted adamantane compounds, pharmaceutical compositions thereof, processes for their preparation, and methods for inhibiting sphingosine kinase and for treating or preventing hyperproliferative disease, inflammatory disease, or angiogenic disease.Type: ApplicationFiled: October 19, 2011Publication date: April 19, 2012Applicant: APOGEE BIOTECHNOLOGY CORPORATIONInventors: Charles D. Smith, Kevin J. French, Yan Zhuang
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Patent number: 8158560Abstract: The present invention relates to novel arylpyrrolines having the formula (I) and their use as insecticides, as well as to processes for the preparation of the arylpyrrolines wherein L, A1 to A4, Y1 to Y3, R1 to R3 are as defined in the specification of the patent application.Type: GrantFiled: November 8, 2010Date of Patent: April 17, 2012Assignee: Bayer CropScience AGInventors: Tetsuya Murata, Masashi Ataka, Yasushi Yoneta, Hidekazu Watanabe, Eiichi Shimojo, Katsuhiko Shibuya, Teruyuki Ichihara
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Patent number: 8158673Abstract: This invention is directed to a compound of formula I, as defined herein, or a pharmaceutically acceptable salt thereof; a pharmaceutical composition containing a compound of formula I, a process of preparation of a compound of formula I, a method of treatment of a disorder or condition that may be treated by antagonizing histamine H3 receptors, the method comprising administering to a mammal in need of such treatment a compound of formula I as described above, and a method of treatment of a disorder or condition selected from the group consisting of depression, mood disorders, schizophrenia, anxiety disorders, Alzheimer's disease, attention-deficit hyperactivity disorder (ADHD), psychotic disorders, cognitive disorders, sleep disorders, obesity, dizziness, epilepsy, motion sickness, respiratory diseases, allergy, allergy-induced airway responses, allergic rhinitis, nasal congestion, allergic congestion, congestion, hypotension, cardiovascular disease, diseases of the GI tract, hyper and hypo motility andType: GrantFiled: October 13, 2006Date of Patent: April 17, 2012Assignee: Pfizer Inc.Inventors: Travis T. Wager, Ramalakshmi Y Chandrasekaran, Todd William Butler
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Publication number: 20120088799Abstract: In one aspect, the invention relates to compounds of formula I: where X, Y, R1, R2, R3, R4, R4, and n are as defined in the specification, or a pharmaceutically acceptable salt thereof. The compounds of formula I are serotonin reuptake inhibitors. In another aspect, the invention relates to pharmaceutical compositions comprising such compounds; methods of using such compounds; and process and intermediates for preparing such compounds.Type: ApplicationFiled: October 10, 2011Publication date: April 12, 2012Applicant: THERAVANCE, INC.Inventors: Eric L. STANGELAND, Lori Jean PATTERSON, Daisuke Roland SAITO
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Patent number: 8147809Abstract: Soft anticholinergic esters of the formulas: wherein R1 and R2 are both phenyl or one of R1 and R2 is phenyl and the other is cyclopentyl; R is C1-C8 alkyl, straight or branched chain; and X? is an anion with a single negative charge; and wherein each asterisk marks a chiral center; said compound having the R, S or RS stereoisomeric configuration at each chiral center unless specified otherwise, or being a mixture thereof.Type: GrantFiled: June 30, 2009Date of Patent: April 3, 2012Inventor: Nicholas S. Bodor
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Patent number: 8129547Abstract: The present invention relates to a method for the anticoagulation of human blood ex vivo in which blood calcium concentration remains the same, no thrombin is formed and thrombocyte function is not affected. The invention further relates to a blood coagulation factor Xa inhibitor that can be advantageously used in this method, an agent that contains an inhibitor of the blood coagulation factor Xa, and a kit for diagnosing cellular blood components. The anticoagulated blood obtained according to the invention can be used for examining cellular blood components, for example for the diagnosis of thrombocyte function.Type: GrantFiled: January 26, 2007Date of Patent: March 6, 2012Inventors: Peter Hellstern, Jörg Stürzebecher, Uta Stürzebecher, legal representative
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Publication number: 20120052118Abstract: The present invention provides an apparatus and process for making softgel capsules having incorporated therein other solid dosage forms selected from the group consisting of pellets, smaller capsules, smaller tablets, sustained release solid dosage forms, immediate release solid dosage forms, extended release solid dosage forms and zero order release solid dosage forms, said apparatus comprising: (a) two spreader boxes; (b) two casting drums; (c) a pair of rotary dies having means for suction; (d) a liquid fill system; (e) a wedge for heating gelatine ribbons and feeding said fill; and (f) two lateral dispensing devices said lateral dispensing devices including hoppers having said solid dosage forms, channelguides for transporting said solid dosage forms and a grasping claw for dispensing said solid dosage form into the softgel pocket formed in the rotary dies.Type: ApplicationFiled: July 18, 2011Publication date: March 1, 2012Inventors: Carlos Salazar Altamar, Gustavo Anaya, Braulio Teran, Newman Aguas Navarro, Willmer Herrera
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Publication number: 20120052019Abstract: Chemical entities which are triterpenoid derivatives, pharmaceutical compositions and methods of treatment of inflammatory, neurodegenerative, neoplastic and autoimmune diseases are described.Type: ApplicationFiled: August 22, 2011Publication date: March 1, 2012Inventors: Xiangping Qian, Yong-Liang Zhu
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Publication number: 20120053222Abstract: The invention relates to the prevention and treatment of metabolic abnormalities characterized by abnormal glucose metabolism, including diabetes mellitus and new onset diabetes mellitus through the use of fibroblast activation protein (FAP) selective inhibitors.Type: ApplicationFiled: January 22, 2010Publication date: March 1, 2012Inventors: Mark Gorrell, Sunmi Song, Xin Wang
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Publication number: 20120027871Abstract: The invention provides methods for the administration of compounds capable of prolonging a QTc interval and methods for predicting whether an individual is predisposed to such QTc prolongation.Type: ApplicationFiled: April 5, 2010Publication date: February 2, 2012Applicant: VANDA PHARMACEUTICALS, INC.Inventors: Curt D. Wolfgang, Mihael H. Polymeropoulos
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Patent number: 8106090Abstract: The present invention is directed to compounds of formula (I): or a pharmaceutically acceptable salt thereof; wherein A is (II); X is selected from CH, CF and N, R8 is selected from H, C1-C6 alkyl, aryl, heteroaryl, C1-C6 alkylaryl, C1-C6 alkylheteroaryl, C2-C6 alkyl-O—C1-C6 alkyl, C1-C6 haloalkyl, hydroxy C2-C6 alkyl, —C(O)R9 and —SO2R9, or R7 and R8 combine to form (III), (IV); W is selected from CR1O and CR15, R1O is selected from H, halo, —C(O)NR13R14, C1-C6 alkyl, aryl, heteroaryl, C1-C6 alkylaryl, C1-C6 alkylheteroaryl, C1-C6 alkyl-O—C1-C6 alkyl and hydroxy C1-C6 alkyl; Het is a N-linked 5-membered heteroaryl ring optionally substituted with 1-3 substituents selected from methoxy, Cl, F, CH3, CF3, aryl, heteroaryl, C1-C4 alkylaryl or C1-C4 alkylheteroaryl, for use as inhibitors of the DPP-IV enzyme in the treatment or prevention of conditions including Type II diabetes.Type: GrantFiled: July 14, 2006Date of Patent: January 31, 2012Assignee: Eli Lilly and CompanyInventors: Larry Chris Blaszczak, Shon Roland Pulley, Michael Alan Robertson, Scott Martin Sheehan, Qing Shi, Michael Robert Wiley
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Publication number: 20120010265Abstract: The invention provides a crystalline hydrochloride salt of (S)-3-[(S)-1-(4-chlorophenoxy)-2-methylpropyl]pyrrolidine. This invention also provides pharmaceutical compositions comprising the crystalline salt, processes and intermediates for preparing the crystalline salt, and methods of using the crystalline salt to treat diseases.Type: ApplicationFiled: June 30, 2011Publication date: January 12, 2012Inventors: Daisuke Roland SAITO, Miroslav RAPTA
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Publication number: 20120004225Abstract: The present invention provides bumetanide, furosemide, piretanide, azosemide, and torsemide analogs and compositions comprising such analogs. The present invention also provides pharmaceutical compositions containing these bumetanide, furosemide, piretanide, azosemide, and torsemide analogs and methods for their use. All of these analogs are particularly useful for the treatment and/or prophylaxis of conditions that involve the Na+K+Cl? co-transporter or GABAA receptor including but not limited to addictive disorders, Alzheimer's Disease, anxiety disorders, ascites, autism, bipolar disorder, cancer, depression, endothelial corneal dystrophy, edema, epilepsy, glaucoma, Huntington's Disease, insomnia, ischemia, migraine, migraine with aura, neuropathic pain, nociceptive neuralgia, nociceptive pain, ocular diseases, pain, Parkinson's disease, personality disorders, postherpetic neuralgia, psychosis, schizophrenia, seizure disorders, tinnitus, and withdrawal syndromes.Type: ApplicationFiled: January 22, 2010Publication date: January 5, 2012Applicant: NeuroTherapeutics Pharma, Inc.Inventors: Stephen Wanaski, John J. Partridge, Stephen D. Collins
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Publication number: 20120004264Abstract: 4-(trifluoromethanesulfonyloxyphenyl)propionic acid derivatives and pharmaceutical composition containing such compounds are useful in inhibiting the chemotactic activation of neutrophils (PMN leukocytes) induced by the interaction of Interleukin-8 (IL-8) with CXCR1 and CXCR2 membrane receptors. The compounds are used for the prevention and treatment of pathologies deriving from said activation. Notably, these metabolites are devoid of cyclo-oxygenase inhibition activity and are particularly useful in the treatment of neutrophil-dependent pathologies such as psoriasis, ulcerative colitis, melanoma, chronic obstructive pulmonary disease (COPD), bullous pemphigoid, rheumatoid arthritis, idiopathic fibrosis, glomerulonephritis and in the prevention and treatment of damages caused by ischemia and reperfusion.Type: ApplicationFiled: September 15, 2011Publication date: January 5, 2012Applicant: Dompé pha.r.ma S.p.A.Inventors: Marcello Allegretti, Marla Candida Cesta, Riccardo Bertini, Marco Mosca, Francesco Colotta
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Publication number: 20120004220Abstract: Provided herein are compounds of formulae I to II that bind to androgen receptors and/or modulate activity of androgen receptors; and to methods for making and using such compounds. Also provided are compositions including such compounds and methods for making and using such compositions.Type: ApplicationFiled: December 12, 2008Publication date: January 5, 2012Inventor: Lin Zhi
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Publication number: 20110319468Abstract: Compounds exhibiting calcium receptor antagonist activity that are safe and orally administrable having Formula (I) or pharmaceutically acceptable salts thereofType: ApplicationFiled: June 23, 2011Publication date: December 29, 2011Applicant: DAIICHI SANKYO COMPANY, LIMITEDInventors: Akira Nakao, Kentoku Gotanda, Kazumasa Aoki, Shimpei Hirano, Yoshiharu Hiruma, Takeshi Shiiki
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Publication number: 20110301129Abstract: Controlled release oral dosage forms are provided for the continuous, sustained administration of a pharmacologically active agent to the upper gastrointestinal tract of a patient in whom the fed mode as been induced. The majority of the agent is delivered, on an extended release basis, to the stomach, duodenum and upper regions of the small intestine, with drug delivery in the lower gastrointestinal tract and colon substantially restricted. The dosage form comprises a matrix of a biocompatible, hydrophilic, erodible polymer with an active agent incorporated therein, wherein the polymer is one that both swells in the presence of water and gradually erodes over a time period of hours, with swelling and erosion commencing upon contact with gastric fluid, and drug release rate primarily controlled by erosion rate.Type: ApplicationFiled: June 3, 2011Publication date: December 8, 2011Applicant: DEPOMED, INC.Inventors: BRET BERNER, JENNY LOUIE-HELM
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Publication number: 20110301133Abstract: The present invention relates to novel synthetic substituted heterocyclic compounds and pharmaceutical compositions containing the same that are capable of inhibiting or antagonizing a family of receptor tyrosine kinases, Tropomysosin Related Kinases (Trk), in particular the nerve growth factor (NGF) receptor, TrkA. The invention further concerns the use of such compounds in the treatment and/or prevention of pain, cancer, restenosis, atherosclerosis, psoriasis, thrombosis, or a disease, disorder or injury relating to dysmyelination or demyelination or the disease or disorder associated with abnormal activities of NGF receptor TrkA.Type: ApplicationFiled: December 8, 2009Publication date: December 8, 2011Applicant: VM Pharma LLCInventors: Jay Jie-Qiang Wu, Ling Wang
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Publication number: 20110301105Abstract: We have discovered that p63 inhibition results in increased cellular proliferation. We have also performed a screen for agents capable of increasing cellular proliferation, (e.g., of stem cells such as skin-derived precursors (SKPs)). The invention therefore invention provides compositions, methods, and kits for increasing proliferation of cells, using compounds that decrease p63 expression or activity or using the compounds described herein. The invention also features methods of using these compounds for increasing hair growth, improving skin health, or promoting skin repair in a subject.Type: ApplicationFiled: March 30, 2011Publication date: December 8, 2011Applicant: The Hospital for Sick ChildrenInventors: Freda Miller, David Kaplan, Kristen Smith, Maryline Paris, Sibel Naska
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Patent number: 8071604Abstract: The present invention is related to chemical compositions, processes for the preparation thereof and uses of the composition. Particularly, the present invention relates to compositions of compounds of Formula (A): wherein Ar, X, Y, R1, R2, R3, and q are as defined herein; and their use in the treatment of diseases, including treatment of sleepiness, promotion of wakefulness, treatment of Parkinson's disease, cerebral ischemia, stroke, sleep apneas, eating disorders, stimulation of appetite and weight gain, treatment of attention deficit hyperactivity disorder (“ADHD”), enhancing function in disorders associated with hypofunctionality of the cerebral cortex, including, but not limited to, depression, schizophrenia, fatigue, in particular, fatigue associated with neurologic disease, such as multiple sclerosis, chronic fatigue syndrome, and improvement of cognitive dysfunction.Type: GrantFiled: November 8, 2007Date of Patent: December 6, 2011Assignees: Cephalon France, Cephalon, Inc.Inventors: Brigitte Lesur, Philippe Louvet, Rabindranath Tripathy
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Publication number: 20110294840Abstract: There is provided a hydrazide compound having a controlling effect on pests represented by the formula (1): wherein, G is a 5-membered heterocyclic group, M is an oxygen atom or a sulfur atom, Q1, Q2, Q3 and Q4 is independently a nitrogen atom, etc., m is an integer of 0 to 5, R2 is an optionally halogenated C1-C6 alkyl group, etc., R5 and R6 are independently an optionally substituted C1-C12 chain hydrocarbon group, etc., and R4 is an optionally substituted C1-C12 chain hydrocarbon group, etc.Type: ApplicationFiled: February 5, 2010Publication date: December 1, 2011Inventors: Hideki Ihara, Koji Kumamoto
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Publication number: 20110294775Abstract: Novel compounds which are useful for treating acute pain, visceral pain, neuropathic pain, inflammatory/pain receptor-mediated pain, tumour pain and headache diseases.Type: ApplicationFiled: August 12, 2008Publication date: December 1, 2011Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Norbert Hauel, Angelo Ceci, Henri Doods, Iris Kauffmann-Hefner, Ingo Konetzki, Annette Schuler-Metz, Rainer Walter
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Patent number: 8067394Abstract: This invention describes novel tricyclic-bis-enone derivatives (TBEs), such as TBE-31, TBE-34, TBE-45 and water-soluble TBEs. The methods of preparing these compounds are also disclosed. The inventors demonstrate the ability of these new TBEs to inhibit proliferation of human myeloma cells, inhibit the induction of iNOS in cells stimulated with interferon-?, induce heme oxygenase-1 (HO-1), induce CD11b expression—a leukemia differentiation marker, inhibit proliferation of leukemia cells, induce apoptosis in human lung cancer, and induce apoptosis in other cancerous cells. The TBEs of this invention are expected to be useful agents for the treatment and prevention of many diseases, including cancer, neurological disorders, inflammation, and pathologies involving oxidative stress.Type: GrantFiled: May 10, 2010Date of Patent: November 29, 2011Assignee: Trustees of Dartmouth CollegeInventors: Tadashi Honda, Chitra Sundararajan, Gordon W. Gribble, Michael B. Sporn, Karen T. Liby
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Publication number: 20110288094Abstract: Compounds of the formula where the variables have the meaning defined in the specification have analgesic and/or immunostimulant effect in mammals.Type: ApplicationFiled: August 2, 2011Publication date: November 24, 2011Applicant: ALLERGAN, INC.Inventors: Bertrand Leblond, Eric Beusoleil, Thierry Taverne, John E. Donello
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Patent number: 8063098Abstract: The present invention relates to a compound of formula I wherein R1, R2, X, Ar1 and Ar2 are as defined herein and to pharmaceutically acceptable acid addition salts, to a racemic mixtures, or to their corresponding enantiomers and/or optical isomers thereof. Compounds of the invention are good inhibitors of the glycine transporter 1 (GlyT-1), and have a good selectivity to glycine transporter 2 (GlyT-2) inhibitors.Type: GrantFiled: August 14, 2009Date of Patent: November 22, 2011Assignee: Hoffmann-La Roche Inc.Inventors: Sabine Kolczewski, Robert Narquizian, Emmanuel Pinard
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Patent number: 8058475Abstract: Novel cyclohexylmethyl compounds corresponding to formula I wherein R1, R2, R3, R4 and R5, have the meanings given in the description. Pharmaceutical formulations containing these compounds, as well as a processes for preparing these compounds and related methods of treatment are also provided.Type: GrantFiled: June 20, 2008Date of Patent: November 15, 2011Assignee: Gruenenthal GmbHInventors: Stefan Oberboersch, Beatrix Merla, Bernd Sundermann, Werner Englberger, Hagen-Heinrich Hennies, Achim Kless, Petra Bloms-Funke, Babette-Yvonne Koegel, Heinze Graubaum
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Publication number: 20110275694Abstract: In one aspect, the invention relates to compounds of formula I: where a and R1-6 are as defined in the specification, or a pharmaceutically acceptable salt thereof. The compounds of formula I are serotonin and norepinephrine reuptake inhibitors. In another aspect, the invention relates to pharmaceutical compositions comprising such compounds; methods of using such compounds; and process and intermediates for preparing such compounds.Type: ApplicationFiled: January 4, 2011Publication date: November 10, 2011Applicant: THERAVANCE, INC.Inventors: Eric Stangeland, Priscilla Van Dyke, Timothy J. Church, Lori Jean Patterson, Daisuke Roland Saito
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Publication number: 20110275615Abstract: An amide of the formula I and its tautomeric forms, possible enantiomeric and diastereomeric forms, E and Z forms, and possible physiologically tolerated salts, in which the variables have the following meanings: A —(CH2)p—R1, where R1 can be pyrrolidine, morpholine, piperidine, —NR5R6 and and R5, R6 and R7 can, independently of one another, be hydrogen, C1-C4-alkyl, CH2Ph, Ph, CH2CH2Ph, it also being possible for the phenyl rings to be substituted by R6, and p can be 1 and 2, and B can be phenyl, pyridyl, pyrimidyl and pyridazyl, it also being possible for the rings to be substituted by up to 2 R8 radicals, and D can be a bond, —(CH2)m—, —CH?CH—, —C?C—, and R2 is chlorine, bromine, fluorine, C1-C6-alkyl, NHCO—C1-C4-alkyl, NHSO2—C1-C4-alkyl, NO2, —O—C1-C4-alkyl and NH2, and R3 is —C1-C6-alkyl, branched or unbranched, and which may also carry a phenyl ring, indolyl ring or cyclohexyl ring which is in turn substituted by a maximum of two R8 radicals, where R8 is hydrogen, C1-C4-alkyl, branched or unType: ApplicationFiled: October 29, 2010Publication date: November 10, 2011Inventors: Hans-Jörg Treiber, Monika Knopp, Wilfried Lubisch, Achim Moeller
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Publication number: 20110268820Abstract: Methods for facilitating joint immobilization or fusion using selective estrogen receptor modulator (SERM) such as raloxifene are disclosed. The SERM may be administered systemically or locally. In conjunction with SERM, other therapeutic agents such as calcium, vitamin D, bone morphogenetic protein may be administered simultaneously. The method can similarly be applied to facilitate bone repair, bone healing, and connective tissue healing processes in a patient.Type: ApplicationFiled: April 30, 2010Publication date: November 3, 2011Inventor: John G. Stark
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Patent number: 8048908Abstract: The use of substituted amides for modulating the activity of 11?-hydroxysteroid dehydrogenase type 1 (11?HSD1) and the use of these compounds as pharmaceutical compositions, are described. Also a novel class of substituted amides, of the general formula I. Their use in therapy, pharmaceutical compositions comprising the compounds, as well as their use in the manufacture of medicaments are described. The present compounds are modulators and more specifically inhibitors of the activity of 11?HSDI and may be useful in the treatment of a range of medical disorders where a decreased intracellular concentration of active glucocorticoid is desirable.Type: GrantFiled: June 28, 2007Date of Patent: November 1, 2011Assignee: High Point Pharmaceuticals, LLCInventors: Soren Ebdrup, Henrik Sune Andersen
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Patent number: 8048910Abstract: Novel combinations based on anticholinergics, ?2-adrenoceptor agonists, PDE 4 Inhibitors, glucocorticoids, and leukotriene-receptor antagonists, process for their production and their use for the treatment of inflammatory diseases, preferably respiratory diseases as bronchial asthma and chronic obstructive pulmonary diseases (COPD) or rheumatic or autoimmune diseases. A particular combination comprises R,R-glycopyrrolate, rolipram, and budesonide, or physiologically acceptable salts thereof, wherein dosage amounts are such that a synergistic therapeutic effect is achieved.Type: GrantFiled: December 21, 2006Date of Patent: November 1, 2011Assignee: Meda Pharma GmbH & Co. KGInventors: Joachim Maus, Horst Kastrup, Istvan Szelenyi, Peter Jürgen Cnota, Artur Bauhofer
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Publication number: 20110263556Abstract: This invention relates to compounds of formula I, their use as inhibitors of the microsomal prostaglandin E2 synthase-1 (mPGES-1), pharmaceutical compositions containing them, and their use as medicaments for the treatment and/or prevention of inflammatory diseases and associated conditions such as inflammatory/nociceptive pain. A, M, R1, R2, R7, Ra, Rb, Q3, Q4, Q6, Z2, Z4, Z5, Z6 and W have meanings given in the description.Type: ApplicationFiled: October 20, 2010Publication date: October 27, 2011Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Henning PRIEPKE, Henri DOODS, Raimund KUELZER, Roland PFAU, Dirk STENKAMP, Robert ROENN, Benjamin PELCMAN
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Publication number: 20110263554Abstract: The invention provides methods to identify agents useful to prevent, inhibit or treat viral infections, e.g. filovirus infections, as well as compositions having one or more agents to prevent, inhibit or treat viral infection.Type: ApplicationFiled: November 6, 2009Publication date: October 27, 2011Applicant: WARF - Wisconsin Alumni Research FoundationInventors: Yoshihiro Kawaoka, Shinji Watanabe, Yasuko Hatta
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Patent number: 8044048Abstract: Derivatives of sulindac are provided along with pharmaceutical compositions containing them and use for precancerous conditions and treating cancer. Derivatives of sulindac are also suitable for treating chronic inflammatory conditions. A method for preparing the derivatives is also provided.Type: GrantFiled: January 4, 2007Date of Patent: October 25, 2011Assignee: Southern Research InstituteInventors: Gary Piazza, Robert Reynolds
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Publication number: 20110257243Abstract: In one aspect, the invention relates to compounds of formula I: where R1-6 are as defined in the specification, or a pharmaceutically acceptable salt thereof. The compounds of formula I are serotonin and norepinephrine reuptake inhibitors. In another aspect, the invention relates to pharmaceutical compositions comprising such compounds; methods of using such compounds; and process and intermediates for preparing such compounds.Type: ApplicationFiled: June 30, 2011Publication date: October 20, 2011Applicant: THERAVANCE, INC.Inventors: Eric Stangeland, Daisuke Roland Saito, Adam Hughes, Jane Schmidt, Priscilla Van Dyke, Lori Jean Patterson
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Patent number: 8039656Abstract: 4-(trifluoromethanesulfonyloxyphenyl)propionic acid derivatives and pharmaceutical composition containing such compounds are useful in inhibiting the chemotactic activation of neutrophils (PMN leukocytes) induced by the interaction of Interleukin-8 (IL-8) with CXCR1 and CXCR2 membrane receptors. The compounds are used for the prevention and treatment of pathologies deriving from said activation. Notably, these metabolites are devoid of cyclo-oxygenase inhibition activity and are particularly useful in the treatment of neutrophil-dependent pathologies such as psoriasis, ulcerative colitis, melanoma, chronic obstructive pulmonary disease (COPD), bullous pemphigoid, rheumatoid arthritis, idiopathic fibrosis, glomerulonephritis and in the prevention and treatment of damages caused by ischemia and reperfusion.Type: GrantFiled: March 21, 2005Date of Patent: October 18, 2011Inventors: Marcello Allegretti, Maria Candida Cesta, Riccardo Bertini, Marco Mosca, Francesco Colotta
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Publication number: 20110251196Abstract: The present disclosure is generally directed to compounds which can modulate G-protein coupled receptor 88, compositions comprising such compounds, and methods for modulating G-protein coupled receptor 88.Type: ApplicationFiled: October 5, 2010Publication date: October 13, 2011Inventors: Carolyn Diane Dzierba, Richard A. Hartz, Yingzhi Bi, Vijay T. Ahuja, Joanne J. Bronson, Kenneth Carson, Giovanni Cianchetta, Michael Green, David Kimball, S. Roy Kimura, Soojin Kwon, John E. Macor, Yulian Zhang, Greg Zipp
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Patent number: 8030344Abstract: 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. One aspect of the invention provides compounds of formula (1): in which T, A and X are as described herein.Type: GrantFiled: March 6, 2008Date of Patent: October 4, 2011Assignee: MethylGene Inc.Inventors: Sylvie Frechette, Lubo Isakovic, Isabelle Paquin, Simon Roy, Oscar Moradei, Arkadii Vaisburg
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Publication number: 20110230540Abstract: Provided are manassantin compounds and methods of using the compounds. Provided are methods of treating a disease, the method comprising administering a compound according to Formula I. Further provided are pharmaceutical compositions comprising compounds according to Formula I. Also provided are methods of inhibiting HIF-1 in a cell, the methods comprising administering to the cell a compound according to Formula I.Type: ApplicationFiled: November 19, 2009Publication date: September 22, 2011Applicant: DUKE UNIVERSITYInventors: Jiyong Hong, Mark Dewhirst, Hyoungsu Kim, Amanda C. Kasper, Eui Jung Moon, Yongho Park, Ceshea M. Wooten
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Publication number: 20110224213Abstract: The invention relates to the use of glutaric acid derivatives of general formula (I), which are disclosed in the invention description, as anti-arrhythmic agents.Type: ApplicationFiled: March 18, 2009Publication date: September 15, 2011Inventors: Vladimir Evgenievich Nebolsin, Dmitry Sergeevich Blinov, Vladimir Pavlovich Balashov, Tatyana Alexandrovna Kromova, Galina Alexandrovna Zheltukhina
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Publication number: 20110224256Abstract: The invention features methods, kits, and compositions for the treatment of psychiatric disorders using therapeutic imprinting in pre-pubescent subjects.Type: ApplicationFiled: June 12, 2009Publication date: September 15, 2011Inventor: Susan L. Andersen
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Patent number: 8017633Abstract: The invention relates to the use of Roflumilast and/or Roflumilast N-Oxide for the treatment of diabetes mellitus and accompanying disorders thereof. The invention additionally relates to combinations of Roflumilast and/or Roflumilast N-Oxide with other active agents for the treatment of diabetes mellitus.Type: GrantFiled: March 3, 2006Date of Patent: September 13, 2011Assignee: Nycomed GmbHInventors: Hans-Peter Kley, Guido Hanauer, Daniela Hauser, Beate Schmidt, Dirk Bredenbroeker, Wilhelm Wurst, Joerg Kemkowski
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Patent number: RE43390Abstract: The present invention relates to pleuromutilin derivatives, to processes for their preparation, to pharmaceutical compositions containing them and to their use in medical therapy, particularly antibacterial therapy.Type: GrantFiled: October 27, 1998Date of Patent: May 15, 2012Assignees: GlaxoSmithKline LLC, SmithKline Beecham LimitedInventors: Valerie Joan Berry, Steven Dabbs, Colin Henry Frydrych, Eric Hunt, Francis Dominic Sanderson, Gary Woodnutt