Quinuclidines (including Unsaturation) Patents (Class 514/305)
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Publication number: 20100184727Abstract: A muscarinic receptor antagonist is useful for the treatment or prevention of a condition associated with excess sebum production or excretion.Type: ApplicationFiled: June 7, 2007Publication date: July 22, 2010Applicant: SUMMIT (CAMBRIDGE) LIMITEDInventors: Alan Geoffrey Roach, Paul Goldsmith
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Patent number: 7759361Abstract: Compounds of Formula (1) process for preparing them, pharmaceutical compositions comprising them. The use of compounds of formula (1) for hyperproliferative diseases, e.g. cancer as well as autoimmune diseases and heart disease.Type: GrantFiled: March 22, 2005Date of Patent: July 20, 2010Assignee: Aprea ABInventors: Jacob Westman, Klas Wiman, Galina Selivanova, Vladimir Bykov
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Publication number: 20100173880Abstract: Alkaloid aminoester compounds which act as muscarinic receptor antagonists are useful for the prevention and/or treatment of a broncho-obstructive or inflammatory diseases.Type: ApplicationFiled: December 22, 2009Publication date: July 8, 2010Applicant: Chiesi Farmaceutici S.p.A.Inventors: Antonio Caligiuri, Mauro Riccaboni, Gabriele Amari
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Patent number: 7750022Abstract: This invention relates to novel quinuclidine derivatives and their use as pharmaceuticals. Due to their pharmacological profile the compounds of the invention may be useful for the treatment of diseases or disorders as diverse as those related to the cholinergic system of the central nervous system (CNS), the peripheral nervous system (PNS), diseases or disorders related to smooth muscle contraction, endocrine diseases or disorders, diseases or disorders related to neuro-degeneration, diseases or disorders related to inflammation, pain, and withdrawal symptoms caused by the termination of abuse of chemical substances.Type: GrantFiled: June 29, 2004Date of Patent: July 6, 2010Assignees: Neurosearch A/S, Abbott LaboratoriesInventors: Dan Peters, Gunnar M. Olsen, Elsebet Østergaard Nielsen, Philip K. Ahring, Tino Dyhring Jørgensen, Michael R. Schrimpf, Kevin B. Sippy
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Patent number: 7750023Abstract: The invention provides 3-(2-hydroxy-2,2-dithien-2-ylacetoxy)-1-(3-phenoxypropyl)-1-azoniabicyclo[2.2.2]octane in salt form, pharmaceutical compositions comprising it, and methods of using it for treatment of respiratory disorders, in association with ?2 agonist.Type: GrantFiled: March 7, 2008Date of Patent: July 6, 2010Inventors: María Dolors Fernandez Forner, María Prat Quiñones, María Antonia Buil Albero
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Publication number: 20100168132Abstract: Compounds of Formula (I) ; in salt or zwitterionic form wherein R1, R2, R3 and R4 have the meanings as indicated in the specification, are useful for treating conditions that are mediated by the muscarinic M3 receptor, especially inflammatory or obstructive airways diseases. Pharmaceutical compositions that contain the compounds and a process for preparing the compounds are also described.Type: ApplicationFiled: March 11, 2010Publication date: July 1, 2010Inventors: Neil John Press, Stephen Paul Collingwood, Urs Baettig, Brian Cox, Sudhakar Devidasrao Garad, Hyungshul Kim, Dimitris Papoutsakis, Simon James Watson
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Publication number: 20100158818Abstract: The present application relates to N-chlorinated cationic compounds of Formula I or a salt thereof, and associated compositions and methods of use as antimicrobial agents.Type: ApplicationFiled: November 6, 2009Publication date: June 24, 2010Inventors: Rakesh K. Jain, Eddy Low, Charles Francavilla, Timothy P. Shiau, Satheesh K. Nair
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Publication number: 20100152233Abstract: The present invention relates to 3-substituted-2-(arylalkyl)-1-azabicycloalkanes, methods of preparing the compounds and methods of treatment using the compounds. The azabicycloalkanes generally are azabicycloheptanes, azabicyclooctanes, or azabicyclononanes. The aryl group in the arylalkyl moiety is a 5- or 6-membered ring heteroaromatic, preferably 3-pyridinyl and 5-pyrimidinyl moieties, and the alkyl group is typically a C1-4 alkyl. The substituent at the 3-position of the 1-azabicycloalkane is a carbonyl group-containing moiety, such as an amide, carbamate, urea, thioamide, thiocarbamate, thiourea or similar functionality. The compounds exhibit activity at nicotinic acetylcholine receptors (nAChRs), particularly the ?7 nAChR subtype, and are useful towards modulating neurotransmission and the release of ligands involved in neurotransmission.Type: ApplicationFiled: January 8, 2010Publication date: June 17, 2010Applicant: Targacept, Inc.Inventors: Anatoly A. Mazurov, Lan Miao
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Publication number: 20100152231Abstract: The present invention relates to a method of treating irritable bowel syndrome with constipation (IBS-c) or irritable bowel syndrome with alternating constipation and diarrhea (IBS-a) in a subject in need of treatment. The method comprises administering to said subject a therapeutically effective amount of a thieno[3,2-b]pyridine compound of Structural Formula I or a pharmaceutically acceptable salt or N-oxide derivative thereof.Type: ApplicationFiled: December 10, 2009Publication date: June 17, 2010Inventors: Steven B. Landau, Suhail Nurbhai
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Publication number: 20100152232Abstract: The present invention relates to 3-substituted-2-(arylalkyl)-1-azabicycloalkanes, methods of preparing the compounds and methods of treatment using the compounds. The azabicycloalkanes generally are azabicycloheptanes, azabicyclooctanes, or azabicyclononanes. The aryl group in the arylalkyl moiety is a 5- or 6-membered ring heteroaromatic, preferably 3-pyridinyl and 5-pyrimidinyl moieties, and the alkyl group is typically a C1-4 alkyl. The substituent at the 3-position of the 1-azabicycloalkane is a carbonyl group-containing moiety, such as an amide, carbamate, urea, thioamide, thiocarbamate, thiourea or similar functionality. The compounds exhibit activity at nicotinic acetylcholine receptors (nAChRs), particularly the ?7 nAChR subtype, and are useful towards modulating neurotransmission and the release of ligands involved in neurotransmission.Type: ApplicationFiled: December 11, 2009Publication date: June 17, 2010Applicant: Targacept, Inc.Inventors: Anatoly A. Mazurov, Lan Miao
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Publication number: 20100143347Abstract: The present invention concerns protection of an organ or tissue following an ischemic episode In particular aspects, the invention concerns organ preservation for transplantation, angina pectoris, kidney reperfusion injury, and so forth In specific embodiments, the organ is subjected to an inhibitor of an NCCa-ATP channel that is regulated by SUR1 Exemplary inhibitors include sulfonylurea compounds, such as glibenclamide, for exampleType: ApplicationFiled: January 11, 2008Publication date: June 10, 2010Inventor: J. Marc Simard
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Publication number: 20100137288Abstract: The present invention relates generally to the field of ligands for nicotinic acetylcholine receptors (nACh receptors), activation of nACh receptors, and the treatment of disease conditions associated with defective or malfunctioning nicotinic acetylcholine receptors, especially of the brain. Further, this invention relates to novel compounds (e.g., indazoles and benzothiazoles), which act as ligands for the ?7 nACh receptor subtype, methods of preparing such compounds, compositions containing such compounds, and methods of use thereof.Type: ApplicationFiled: February 5, 2010Publication date: June 3, 2010Inventors: Richard Schumacher, Mihaela Diana Danca, Jianguo Ma, Brian Herbert, True Minh Nguyen, Wenge Xie, Ashok Tehim
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Publication number: 20100136096Abstract: Certain embodiments disclosed relate to compositions, including therapeutic compositions, methods, devices, and systems that modulate at least one inflammatory response or reaction. According to various embodiments, the compositions, methods, devices, and systems relate to modulating one or more of Toll-like receptors, Src family kinases, NF-kB molecules, proteases, or proteasomes.Type: ApplicationFiled: December 2, 2008Publication date: June 3, 2010Inventors: Roderick A. Hyde, Stephen L. Malaska, Elizabeth A. Sweeney, Lowell L. Wood,, JR.
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Publication number: 20100135983Abstract: Certain embodiments disclosed relate to compositions, including therapeutic compositions, methods, devices, and systems that modulate at least one inflammatory response or reaction. According to various embodiments, the compositions, methods, devices, and systems relate to modulating one or more of Toll-like receptors, Src family kinases, NF-kB molecules, proteases, or proteasomes.Type: ApplicationFiled: December 2, 2008Publication date: June 3, 2010Inventors: Roderick A. Hyde, Stephen L. Malaska, Elizabeth A. Sweeney, Lowell L. Wood, JR.
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Publication number: 20100136094Abstract: Certain embodiments disclosed relate to compositions, including therapeutic compositions, methods, devices, and systems that modulate at least one inflammatory response or reaction. According to various embodiments, the compositions, methods, devices, and systems relate to modulating one or more of Toll-like receptors, Src family kinases, NF-kB molecules, proteases, or proteasomes.Type: ApplicationFiled: December 2, 2008Publication date: June 3, 2010Inventors: Roderick A. Hyde, Stephen L. Malaska, Elizabeth A. Sweeney, Lowell L. Wood, JR.
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Publication number: 20100137358Abstract: Compositions and/or formulations comprising solifenacin or a salt thereof and processes for preparing the same. Certain compositions and formulations contain a stable amorphous form of solifenacin succinate.Type: ApplicationFiled: April 11, 2008Publication date: June 3, 2010Applicants: DR. REDDY'S LABORATORIES LTD., DR. REDDY'S LABORATORIES, INC.Inventors: Pramod Kharwade, Movva Snehalatha, Atul Vishvanath Patil, Narayanan Badri Vishwanathan, Indu Bhushan, Venkata Nookaraju Sreedharala, Harshal Prabhakar Bhagwatwar, Surya Narayana Devarakonda, Ravi Kumar Komareddy, Azeezulla Baig Mohammed, Arjun Kumar Tummala, Jaydeepkumar Dahyabhai Lilakar, Srirami Reddy Kikkuru, Swarupa Dudipala
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Publication number: 20100135984Abstract: Certain embodiments disclosed relate to compositions, including therapeutic compositions, methods, devices, and systems that modulate at least one inflammatory response or reaction. According to various embodiments, the compositions, methods, devices, and systems relate to modulating one or more of Toll-like receptors, Src family kinases, NF-kB molecules, proteases, or proteasomes.Type: ApplicationFiled: December 2, 2008Publication date: June 3, 2010Inventors: Roderick A. Hyde, Stephen L. Malaska, Elizabeth A. Sweeney, Lowell L. Wood, JR.
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Publication number: 20100136097Abstract: Certain embodiments disclosed relate to compositions, including therapeutic compositions, methods, devices, and systems that modulate at least one inflammatory response or reaction. According to various embodiments, the compositions, methods, devices, and systems relate to modulating one or more of Toll-like receptors, Src family kinases, NF-kB molecules, proteases, or proteasomes.Type: ApplicationFiled: December 2, 2008Publication date: June 3, 2010Inventors: Roderick A. Hyde, Stephen L. Malaska, Elizabeth A. Sweeney, Lowell L. Wood, JR.
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Publication number: 20100137246Abstract: Certain embodiments disclosed relate to compositions, including therapeutic compositions, methods, devices, and systems that modulate at least one inflammatory response or reaction. According to various embodiments, the compositions, methods, devices, and systems relate to modulating one or more of Toll-like receptors, Src family kinases, NF-kB molecules, proteases, or proteasomes.Type: ApplicationFiled: December 2, 2008Publication date: June 3, 2010Inventors: Roderick A. Hyde, Stephen L. Malaska, Elizabeth A. Sweeney, Lowell L. Wood, JR.
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Publication number: 20100137247Abstract: Certain embodiments disclosed relate to compositions, including therapeutic compositions, methods, devices, and systems that modulate at least one inflammatory response or reaction. According to various embodiments, the compositions, methods, devices, and systems relate to modulating one or more of Toll-like receptors, Src family kinases, NF-kB molecules, proteases, or proteasomes.Type: ApplicationFiled: December 2, 2008Publication date: June 3, 2010Inventors: Roderick A. Hyde, Stephen L. Malaska, Elizabeth A. Sweeney, Lowell L. Wood, JR.
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Publication number: 20100136095Abstract: Certain embodiments disclosed relate to compositions, including therapeutic compositions, methods, devices, and systems that modulate at least one inflammatory response or reaction. According to various embodiments, the compositions, methods, devices, and systems relate to modulating one or more of Toll-like receptors, Src family kinases, NF-kB molecules, proteases, or proteasomes.Type: ApplicationFiled: December 2, 2008Publication date: June 3, 2010Inventors: Roderick A. Hyde, Stephen L. Malaska, Elizabeth A. Sweeney, Lowell L. Wood, JR.
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Patent number: 7723356Abstract: Compounds of Formula (I); in salt or zwitterionic form wherein R1, R2, R3 and R4 have the meanings as indicated in the specification, are useful for treating conditions that are mediated by the muscarinic M3 receptor, especially inflammatory or obstructive airways diseases. Pharmaceutical compositions that contain the compounds and a process for preparing the compounds are also described.Type: GrantFiled: October 31, 2005Date of Patent: May 25, 2010Assignee: Novartis AGInventors: Neil John Press, Stephen Paul Collingwood, Urs Baettig, Brian Cox, Sudhakar Devidasrao Garad, Hyungchul Kim, Dimitris Papoutsakis, Simon James Watson
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Publication number: 20100125063Abstract: Combinations which comprise at least one nicotinic acetylcholine alpha 7 receptor agonist and at least one compound selected from the group consisting of (a) conventional antipsychotics (b) atypical antipsychotics (c) cognition, attention and/or memory enhancers (d) and to use of these combinations in the treatment of psychiatric disorders.Type: ApplicationFiled: January 20, 2010Publication date: May 20, 2010Inventors: Hans O. KALKMAN, Joachim NOZULAK, Annick VASSOUT, Konstanze HURTH, Dominik FEUERBACH, Conrad GENTSCH, Graeme BILBE
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Patent number: 7718670Abstract: New quinuclidine amide derivatives having the chemical structure of general formula (I) and pharmaceutically acceptable salts thereof including quaternary salts of formula (II) are disclosed; as well as processes for their preparation, pharmaceutical compositions comprising them and their use in therapy as antagonists of M3 muscarinic receptors.Type: GrantFiled: January 8, 2008Date of Patent: May 18, 2010Assignee: Laboratorios Almirall S.AInventor: Maria Prat Quinones
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Publication number: 20100120770Abstract: The invention provides compounds of formula I and pharmaceutically acceptable salts thereof. The formula I thiazolyl compounds inhibit tyrosine kinase activity thereby making them useful as anticancer agents and for the treatment of Alzheimer's disease.Type: ApplicationFiled: April 9, 2008Publication date: May 13, 2010Inventors: Anne Marinier, Marco Dodier, Stephan Roy, Kurt Zimmermann, Xiaopeng Sang, Mark D. Wittman, David R. Langley, Ramkumar Rajamani
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Publication number: 20100120842Abstract: The instant disclosure describes methods for treating diseases and conditions of the central and peripheral nervous system by stimulating or increasing neurogenesis. The disclosure includes compositions and methods based on muscarinic receptor modulation, such as via inhibition of acetylcholine esterase (AChE) activity, alone or in combination with another neurogenic agent to stimulate or activate the formation of new nerve cells.Type: ApplicationFiled: January 22, 2010Publication date: May 13, 2010Applicant: BrainCells, Inc.Inventors: Carrolee Barlow, Todd A. Carter, Kym I. Lorrain, Jammieson C. Pires, Andrew Morse, Dana Gitnick, Kai Treuner, Alex Broadhead
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Publication number: 20100113508Abstract: The present invention relates to modulators of cystic fibrosis transmembrane conductance regulator (“CFTR”), compositions thereof, and methods therewith. The present invention also relates to methods of treating diseases using modulators of CFTR.Type: ApplicationFiled: October 23, 2009Publication date: May 6, 2010Applicant: Vertex Pharmaceuticals, IncorporatedInventors: Hayley Binch, Lev T.D. Fanning, Dennis Hurley, Urvi Sheth, Alina Silina, Xiaoqing Yang, Martyn Botfield, Peter D.J. Grootenhuis, Fredrick Van Goor, Mehdi Michel Djamel Numa
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Publication number: 20100113469Abstract: This invention concerns compositions for the treatment of Lower Urinary Tract Symptoms (LUTS), and especially LUTS which results from benign prostatic hypertrophy. The compositions of the invention comprise a Beta-3 agonist described below, optionally in combination with a 5-alpha reductase inhibitor, or an NK-1 antagonist or an alpha-1 adrenergic antagonist or an anti-muscarinic agent. The invention also includes compositions comprising a beta-3 agonist and two additional active agents selected from a 5-alpha reductase inhibitor, an NK-1 antagonist, an alpha-1 adrenergic antagonist or an anti-muscarinic agent.Type: ApplicationFiled: March 25, 2008Publication date: May 6, 2010Applicant: MERCK & CO., INC.Inventors: Tara Frenkl, Stuart A. Green, Enan Macintyre, Sander G. Mills
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Publication number: 20100113510Abstract: The invention provides compounds of formula (I) wherein R5 is a group of formula (II) or (III) and R1, R2, R3, R4, R6, a, b, Z, Y and X are as defined in the specification, a process for their preparation, pharmaceutical compositions containing them, a process for preparing pharmaceutical compositions, their use in therapy and intermediates of use in their preparation.Type: ApplicationFiled: December 17, 2007Publication date: May 6, 2010Inventors: Rhonan Ford, Antonio Mete, Ian Millichip, Barry Teobald
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Publication number: 20100113509Abstract: The present invention relates to modulators of cystic fibrosis transmembrane conductance regulator (“CFTR”), compositions thereof, and methods therewith. The present invention also relates to methods of treating diseases using modulators of CFTR.Type: ApplicationFiled: October 23, 2009Publication date: May 6, 2010Applicant: Vertex Pharmaceuticals IncorporatedInventors: Hayley Binch, Lev T.D. Fanning, Martyn Botfield, Peter D.J. Grootenhuis, Fredrick van Goor, Mehdi Michel Djamel Numa
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Publication number: 20100105724Abstract: Amorphous and polymorphic of palonosetron hydrochloride are disclosed that can be characterized by X-ray powder diffraction patterns, thermal properties, purity and methods of manufacture. These forms of palonosetron hydrochloride can be produced from solution or by solid state interconversions. The forms can be used in pharmaceutical formulations: particularly preferred uses of these formulations are in prevention and treatment of nausea and emesis arising from chemotherapy or postoperative side effects. The forms can optionally be used as mixtures of the crystalline and/or amorphous forms.Type: ApplicationFiled: December 4, 2007Publication date: April 29, 2010Applicant: HELSINN HEALTHCARE SAInventors: Waldo Mossi, Giorgio Calderari, Enrico Braglia, Riccardo Braglia, Wilma Timraz, Tai Wah Chan
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Publication number: 20100105658Abstract: [Problems] Provided is a compound which has an antagonistic action on a muscarinic M3 receptor and is useful as an active ingredient of a prophylactic and/or therapeutic agent for an inflammatory disease such as a chronic obstructive pulmonary disease (COPD), asthma and the like. [Means for Solving Problems] The present inventors have made studies on a compound having an antagonistic action on the binding of a muscarinic M3 receptor, and they have found that an aza-bridged-ring compound or a salt thereof has an antagonistic action on the binding of a muscarinic M3 receptor, thereby completing the present invention. The aza-bridged-ring compound of the present invention has an antagonistic action on the binding of a muscarinic M3 receptor, and can be used as a prophylactic and/or therapeutic agent for an inflammatory disease such as a chronic obstructive pulmonary disease (COPD), asthma and the like.Type: ApplicationFiled: February 7, 2008Publication date: April 29, 2010Applicant: ASTELLAS PHARMA INC.Inventors: Shinya Nagashima, Toru Kontani, Hiroshi Nagata, Yuji Matsushima, Hisao Hamaguchi, Tadatsura Koshika
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Publication number: 20100105677Abstract: The present invention relates generally to the field of ligands for nicotinic acetylcholine receptors (nACh receptors), activation of nACh receptors, and the treatment of disease conditions associated with defective or malfunctioning nicotinic acetylcholine receptors, especially of the brain. Further, this invention relates to novel compounds (e.g., indazoles and benzothiazoles), which act as ligands for the ?7 nACh receptor subtype, methods of preparing such compounds, compositions containing such compounds, and methods of use thereof.Type: ApplicationFiled: December 4, 2009Publication date: April 29, 2010Inventors: Wenge Xie, Brian Herbert, Richard A. Schumacher, Truc Minh Nguyen, Jianguo Ma, Carla Maria Gauss, Ashok Tehim
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Patent number: 7705016Abstract: Methods of reducing food intake and glucose production in a mammal, or restoring hepatic autoregulation are provided. The methods involve increasing long-chain fatty acyl-Co-A (LC-CoA) levels in the hypothalamus, or stimulating efferent fibers in the hepatic branch of the vagus nerve. Also provided are methods of increasing food intake and glucose production in a mammal. The methods involve decreasing long-chain fatty acyl-Co-A (LC-CoA) levels in the hypothalamus of the mammal.Type: GrantFiled: February 12, 2004Date of Patent: April 27, 2010Assignee: Albert Einstein College of Medicine of Yeshiva UniversityInventors: Luciano Rossetti, Silvana Obici
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Publication number: 20100099701Abstract: The present invention relates to new isoquinolinone modulators of 5-HT3 receptors, pharmaceutical compositions thereof, and methods of use thereof.Type: ApplicationFiled: October 19, 2009Publication date: April 22, 2010Applicant: AUSPEX PHARMACEUTICALS, INC.Inventor: Thomas G. Gant
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Publication number: 20100093746Abstract: The present invention relates to 1-aza-bicycloalkyl derivatives of formula (I) wherein the substituents are as defined in the specification, to processes for their production, their use as pharmaceuticals in the prevention and treatment of psychotic and neurodegenerative disorders. The claimed compounds act as nicotinic acetylcholine receptors (NACHR) ligands.Type: ApplicationFiled: December 15, 2009Publication date: April 15, 2010Inventors: Dominik FEUERBACH, Mathias FREDERIKSEN, Konstanze HURTH, Bernard Lucien ROY
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Patent number: 7696350Abstract: This invention relates to chromen-2-one derivatives useful as monoamine neurotransmitter re-uptake inhibitors. In other aspects the invention relates to the use of these compounds in a method for therapy and to pharmaceutical compositions comprising the compounds of the invention.Type: GrantFiled: September 28, 2005Date of Patent: April 13, 2010Assignee: Neurosearch A/SInventors: Dan Peters, Gunnar M. Olsen, Jørgen Scheel-Krüger, Elsebet Østergaard Nielsen
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Publication number: 20100080829Abstract: The present invention relates to a new lyophilized pharmaceutical composition capable of adhering to oral mucosal tissue for an extended period of time for delivering active pharmaceutical ingredient through the oral mucosal tissue using transmucosal absorption.Type: ApplicationFiled: October 1, 2009Publication date: April 1, 2010Applicants: CEPHALON FRANCE, CEPHALON, INC.Inventors: Claire Dulieu, Steve Durfee, Richard J. Holl, Tam Nguyen
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Patent number: 7687519Abstract: The invention provides compounds of formula I: wherein a, b, c, m, n, q, r, W, Z1, Ar1, Z2, Y, R1, R2, and R3 are as defined in the specification. The compounds of formula I are muscarinic receptor antagonists. The invention also provides pharmaceutical compositions containing such compounds, processes and intermediates for preparing such compounds and methods of using such compounds to treat pulmonary disorders.Type: GrantFiled: March 9, 2006Date of Patent: March 30, 2010Assignee: Theravance, Inc.Inventors: YongQi Mu, Yu-Hua Ji, Mathai Mammen, Viengkham Malathong
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Patent number: 7683075Abstract: The present invention relates to novel isoquinoline-3-carboxylic acid amides having ?7 nicotinic acetylcholine receptor agonistic activity, their preparation, their use as pharmaceuticals and pharmaceutical compositions containing them.Type: GrantFiled: May 11, 2004Date of Patent: March 23, 2010Assignee: Novartis AGInventor: Max Peter Seiler
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Patent number: 7674794Abstract: Compounds of formula (I) wherein n is 0, 1, or 2; X is O, S, —NH—, and —N-alkyl-; Ar1 is a 6-membered aromatic ring; and Ar2 is a fused bicycloheterocycle. The compounds are useful in treating conditions or disorders prevented by or ameliorated by ?7 nAChR ligands. Also disclosed are pharmaceutical compositions having compounds of formula (I) and methods for using such compounds and compositions.Type: GrantFiled: November 15, 2006Date of Patent: March 9, 2010Assignee: Abbott LaboratoriesInventors: Jianguo Ji, Tao Li
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Publication number: 20100056565Abstract: This invention relates to M3 antagonists of formula (I) wherein R2, R4, R5, R6, W, V, A, D, X, t, u and v are as defined herein; pharmaceutical compositions containing them; methods for their preparation; and their use in the treatment of diseases where enhanced M3 receptor activation is implicated.Type: ApplicationFiled: February 14, 2008Publication date: March 4, 2010Applicant: ARGENTA DISCOVERY LIMITEDInventors: Barbara Giuseppina Avitabile, Harry Finch, Jamie David Knight, Alan John Nadin, Nicholas Charles Ray
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Publication number: 20100048615Abstract: Combinations comprising (a) a PDE4 inhibitor and (b) an antagonist of M3 muscarinic receptors which is 3(R)-(2-hydroxy-2,2-dithien-2-ylacetoxy)-1-(3-phenoxypropyl)-1-azoniabicyclo[2.2.2]octane, in the form of a salt having an anion X, which is a pharmaceutically acceptable anion of a mono or polyvalent acid are useful, e.g., for the treatment of respiratory disease, e.g., asthma or chronic obstructive pulmonary diseases.Type: ApplicationFiled: October 28, 2009Publication date: February 25, 2010Inventors: Jordi Gras Escardo, Jesus Llenas Calvo, Hamish Ryder, Pio Orviz Diaz
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Publication number: 20100048616Abstract: A combination which comprises (a) a PDE4 inhibitor and (b) an antagonist of M3 muscarinic receptors which is (3R)-1-phenethyl-3-(9H-xanthene-9carbonyloxy)-1-azoniabicyclo[2.2.2]octane, in the form of a salt having an anion X, which is a pharmaceutically acceptable anion of a mono or polyvalent acid.Type: ApplicationFiled: October 28, 2009Publication date: February 25, 2010Inventors: Jordi Gras Escardo, Jesus Llenas Calvo, Hamish Ryder, Pio Orviz Diaz
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Publication number: 20100048535Abstract: A method of reducing the concentration of a chemical or drug substance in the blood plasma that targets the same or similar receptors as the normal neurotransmitters in the central or peripheral nervous system includes titrating an initial peak concentration of the chemical or drug substance in the blood for a predefined dosing period, titrating a lowest concentration level of the chemical or drug substance in the blood immediately before the end of the dosing period, and providing a plurality of subsequent dosing periods where each subsequent dosing period requires administration of a dosing amount of the chemical or drug substance and titrating of the peak concentration and the lowest concentration level to ensure that the lowest concentration level of the chemical or drug substance in the blood plasma for the subsequent dosing period is decreased by not more than five percent of the lowest concentration level of the previous dosing period and where the plurality of dosing periods added together extends theType: ApplicationFiled: August 20, 2008Publication date: February 25, 2010Inventors: Kenneth C. Slater, Brenda E. Richardson, Scott M. Connors, Wei-wei Chang
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Publication number: 20100035922Abstract: Quinuclidine carbonate derivatives act as muscarinic receptor antagonists and are effective for the prevention and/or treatment of a broncho-obstructive or inflammatory diseases.Type: ApplicationFiled: July 30, 2009Publication date: February 11, 2010Applicant: Chiesi Farmaceutici S.p.A.Inventors: Gabriele Amari, Maurizio Delcanale
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Patent number: 7659278Abstract: The present invention provides novel compounds, corresponding to formulae I and II, respectively, which are able to reactivate the apoptosis-inducing function of mutant p53 proteins. This reactivation is provided by restoration of sequence-specific DNA-binding activity and transcriptional transactivation function to mutant p53 proteins, and modulation of the conformation-dependent epitopes of the p53 protein. Accordingly, the substances according to the invention will be used in pharmaceutical compositions and methods for treatment of patients suffering from various types of tumours.Type: GrantFiled: February 7, 2003Date of Patent: February 9, 2010Assignee: Aprea ABInventors: Vladimir Bykov, Galina Selivanova, Klas Wiman
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Patent number: 7659282Abstract: Pharmaceutical compositions and methods for treating neurological disorders by administering same are provided. The compositions comprise dextromethorphan in combination with quinidine.Type: GrantFiled: January 12, 2005Date of Patent: February 9, 2010Assignee: Avanir Pharmaceuticals, Inc.Inventors: Gerald Yakatan, James Berg, Laura E. Pope, Richard A. Smith
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Publication number: 20100029713Abstract: The invention provides compounds of formula (I) wherein R4 is a group of formula (II) or (IIIa) or (IIIb) and R1, R2, R3, R5, a, b and X are as defined in the specification, a process for their preparation, pharmaceutical compositions containing them, a process for preparing pharmaceutical compositions, their use in therapy and intermediates of use in their preparation (I), (II), (IIIa), (IIIb).Type: ApplicationFiled: November 13, 2007Publication date: February 4, 2010Applicant: ASTRAZENECA ABInventors: Rhonan Ford, Andrew Mather, Antonio Mete
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Publication number: 20100029712Abstract: A method and solution for perioperatively inhibiting a variety of pain, inflammation, spasm and restenosis processes resulting from cardiovascular or general surgical, therapeutic and diagnostic procedures. The solution preferably includes multiple pain and inflammation inhibitory agents, including at least one local anesthetic agent, and spasm inhibitory agents at dilute concentration in a physiologic carrier, such as saline or lactated Ringer's solution. Specific preferred embodiments of the solution of the present invention for use in cardiovascular and general vascular procedures also include anti-restenosis agents.Type: ApplicationFiled: January 21, 2009Publication date: February 4, 2010Inventors: Gregory A. Demopulos, Pamela Anne Pierce, Jeffrey M. Herz