A Ring Or Polycyclo Ring System In A Substituent E Is Attached Indirectly To The Carboxamide Nitrogen Or To An Amino Nitrogen In Substituent E By Acyclic Nonionic Bonding Patents (Class 514/630)
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Patent number: 7291295Abstract: A method for precipitation of finely divided solid particles comprising a) Dissolving a compound C in a fluid A to provide a solution A; b) Thermostatization of said solution A to a temperature ranging between ?50°0 C. and 200° C.; c) Adding a fluid B to said solution A until a pressure P is obtained, characterized in that said fluid B at a pressure P is miscible with said solution A and acts as a co-solvent to form a solution AB; d) Adding an inert gas to solution AB so as to maintain the pressure P; and e) Reducing the pressure of said solution AB so as to produce the precipitation of said compound C, and wherein the method permits particles of average size less than 20 ?m, with a narrow distribution ranging between 1 and 100 ?m, from a solution, and not a mix, that contains the compound C precipitated.Type: GrantFiled: August 23, 2001Date of Patent: November 6, 2007Assignee: Sociedad Espanola de Carburos Metalicos, S.A.Inventors: Nora Ventosa Rull, Jaume Veciana Miro, Concepción Rovira Angulo, Santiago Sala Verges
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Patent number: 7256204Abstract: A compound of the formula: wherein Ar is an aromatic ring assembly group which may be substituted or a fused aromatic group which may be substituted; X is (i) a bond, (ii) —S—, —SO— or —SO2—, (iii) C1-6 alkylene, C2-6 alkenylene or C2-6 alkynylene, etc.Type: GrantFiled: August 21, 2003Date of Patent: August 14, 2007Assignee: Takeda Pharmaceutical Company LimitedInventors: Kaneyoshi Kato, Jun Terauchi, Hiroaki Fukumoto, Mitsuru Kakihana
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Patent number: 7244767Abstract: The present invention relates to the use of N-acylvanillinamide derivatives capable of activating the peripheral receptor CB1 of cannabinoids. In particular, the present invention relates to the use of compounds of general formula (I) in which the meanings of R, R1, R3 and Y are as defined in the description, for the preparation of a medicinal product which is capable of activating the peripheral receptor CB1 of cannabinoids.Type: GrantFiled: September 27, 2004Date of Patent: July 17, 2007Assignees: Innovet Italia S.R.L., Consiglio Nazionale Delle RichercheInventors: Tiziana Bisogno, Francesco Della Valle, Luciano De Petrocellis, Vincenzo Di Marzo, Gabriele Marcolongo, Dominique Melck
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Patent number: 7223381Abstract: The invention relates to the use of pressurized metered dose inhalers (MDIs) having part or all of their internal surfaces consisting of stainless steel, anodized aluminum or lined with an inert organic coating; and to compositions to be delivered with said MDIs.Type: GrantFiled: September 17, 2002Date of Patent: May 29, 2007Assignee: Chiesi Farmaceutici S.p.A.Inventors: David Lewis, David Ganderton, Brian Meakin, Paolo Ventura, Gaetano Brambilla, Raffaella Garzia
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Patent number: 7179489Abstract: The invention relates to a stable pharmaceutical composition useful in the treatment of respiratory disorders such as asthma, rhinitis and chronic obstructive pulmonary disease (COPD) and a novel micronization process for manufacturing a stable formulation for formoterol or its enantiomers and a carrier/diluent comprising a carbohydrate such as lactose.Type: GrantFiled: May 17, 2001Date of Patent: February 20, 2007Assignee: AstraZeneca ABInventor: Eva Trofast
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Patent number: 7157604Abstract: The present invention relates to compounds and derivatives thereof, their synthesis, and their use as estrogen receptor modulators. The compounds of the instant invention are ligands for estrogen receptors and as such may be useful for treatment or prevention of a variety of conditions related to estrogen functioning including: bone loss, bone fractures, osteoporosis, cartilage degeneration, endometriosis, uterine fibroid disease, hot flashes, increased levels of LDL cholesterol, cardiovascular disease, impairment of cognitive functioning, cerebral degenerative disorders, restenosis, gynecomastia, vascular smooth muscle cell proliferation, obesity, incontinence, and cancer, in particular of the breast, uterus and prostate.Type: GrantFiled: August 9, 2002Date of Patent: January 2, 2007Assignee: Merck & Co., Inc.Inventors: Dongfang Meng, Dann LeRoy Parker, Jr., Robert R. Wilkening, Ronald W. Ratcliffe
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Patent number: 7145036Abstract: A method of preparation of a highly pure salt of R,R-formoterol L-tartrate is disclosed. The process provides the most thermodynamically stable polymorph by recrystallization of a novel polymorph.Type: GrantFiled: February 7, 2005Date of Patent: December 5, 2006Assignee: Sepracor Inc.Inventors: Gerald J. Tanoury, Chris H. Senanayake, Donald W. Kessler
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Patent number: 7115605Abstract: PDF inhibitors and novel methods for their use are provided.Type: GrantFiled: April 5, 2004Date of Patent: October 3, 2006Assignee: SmithKline Beecham CorporationInventors: Kelly M. Aubart, Siegfried B. Christensen, IV, Jacques Briand, Maxwell David Cummings
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Patent number: 7105699Abstract: Treatment of CNS disorders with (1R,4S)-trans 4-(3,4-dichlorophenyl)-1,2,3,4-tetrahydro-1-napthalenamine; and (1S,4R)-trans 4-(3,4-dichlorophenyl)-1,2,3,4-tetrahydro-1-napthalenamine is disclosed. A process for preparing 4-(3,4-dichlorophenyl)-1,2,3,4-tetrahydro-1-napthalenamine is also disclosed. The process includes the preparation of all four isomers of N-[4-(3,4-dichlorophenyl)-1,2,3,4-tetrahydronaphthalen-1-yl]formamide, which are also useful.Type: GrantFiled: September 7, 2005Date of Patent: September 12, 2006Assignee: Sepracor Inc.Inventors: Thomas P. Jerussi, Qun Kevin Fang, Mark G. Currie
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Patent number: 7105701Abstract: Disclosed are multibinding compounds which are ?2-adrenergic receptor agonists and are useful in the treatment and prevention of respiratory diseases such as asthma, bronchitis. They are also useful in the treatment of nervous system injury and premature labor.Type: GrantFiled: May 10, 2005Date of Patent: September 12, 2006Assignee: Theravance, Inc.Inventors: Edmund J. Moran, Seok-Ki Choi
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Patent number: 7087785Abstract: Treatment of CNS disorders with (1R,4S)-trans 4-(3,4-dichlorophenyl)-1,2,3,4-tetrahydro-1-napthalenamine; and (1S,4R)-trans 4-(3,4-dichlorophenyl)-1,2,3,4-tetrahydro-1-napthalenamine is disclosed. A process for preparing 4-(3,4-dichlorophenyl)-1,2,3,4-tetrahydro-1-napthalenamine is also disclosed. The process includes the preparation of all four isomers of N-[4-(3,4-dichlorophenyl)-1,2,3,4-tetrahydronaphthalen-1-yl]formamide, which are also useful.Type: GrantFiled: September 16, 2003Date of Patent: August 8, 2006Assignee: Sepracor Inc.Inventors: Thomas P. Jerussi, Qun Kevin Fang, Mark G. Currie
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Patent number: 7034015Abstract: The invention relates to a novel class of aminobenzophenones derivatives, to pharmaceutical preparations comprising said compounds, to dosage units of such preparations, to methods of treating patients comprising administering said compounds, and to the use of said compounds in the manufacture of pharmaceutical preparations.Type: GrantFiled: August 28, 2002Date of Patent: April 25, 2006Assignee: Leo Pharma A/SInventors: Erik Rytter Ottosen, Anne Marie Horneman, Xifu Liang
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Patent number: 7018618Abstract: An aerosol solution composition for use in an aerosol inhaler comprises an active material, a propellant containing a hydrofluoroalkane, a cosolvent and optionally a low volatility component to increase the mass median aerodynamic diameter (MMAD) of the aerosol particles on actuation of the inhaler. The composition is stabilized by using a small amount of mineral acid and a suitable can having part or all of its internal metallic surfaces made of stainless steel, anodized aluminium or lined with an inert organic coating.Type: GrantFiled: August 14, 2003Date of Patent: March 28, 2006Assignee: Chiesi Farmaceutici S.p.A.Inventors: David Lewis, David Ganderton, Brian Meakin, Gaetano Brambilla, Alessandra Ferraris
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Patent number: 6933320Abstract: An antitumor combination comprising a stilbene derivative and an anticancer compound selected from the group consisting of taxanes, alkylating agents, antimetabolites, vinca alkaloids, platinum compounds, epidophylloptoxins, and antibiotics as the active ingredients is provided. Methods of using these pharmaceutical preparations for the treatment of solid carcinomas and the like are also provided.Type: GrantFiled: March 15, 2002Date of Patent: August 23, 2005Assignee: Aventis Pharma S. A.Inventor: Marie-Christine Bissery
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Patent number: 6888015Abstract: A inhibitor of sphingolipids synthesis comprising a compound represented by general formula A. Desirably, a novel inhibitor of sphingolipids synthesis comprising (1R, 3R) N-(3-hydroxy-1-hydroxymethyl-3-phenylpropyl) alkaneamide, wherein carbon number of alkanoyl group is 8-16. (in the formula, X is an aliphatic alkyl group, desirably is an aliphatic alkyl group having 7 to 15 carbon atoms).Type: GrantFiled: April 19, 2002Date of Patent: May 3, 2005Assignee: Japan Science and Technology AgencyInventors: Shu Kobayashi, Kentaro Hanada
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Patent number: 6870069Abstract: A phenyloxyaniline derivative useful as a ligand for peripheral benzodiazepine receptor having a strong affinity and a high selectivity, which is represented by formula (1): wherein X1 and X2 are same or different and each is hydrogen atom or halogen atom; R1 and R2 are same or different and each is hydrogen atom, an alkyl group having 1 to 10 carbon(s) or a halogen-substituted alkyl group having 1 to 10 carbon(s); and R3 is a halogen-substituted alkyl group having 1 to 5 carbon(s), or a radioisotope thereof.Type: GrantFiled: November 4, 2003Date of Patent: March 22, 2005Assignees: National Institute of Radiological Sciences, Taisho Pharmaceutical Co., Ltd., Nihon Nohyaku Co., Ltd.Inventors: Kazutoshi Suzuki, Ming-Rong Zhang, Tetsuya Suhara, Atsuro Nakazato, Makoto Goto
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Publication number: 20040248985Abstract: The invention provides a novel &bgr;2 adrenergic receptor agonist in crystalline salt form. The invention also provides pharmaceutical compositions comprising the novel &bgr;2 adrenergic receptor agonist in crystalline salt form, formulations containing the pharmaceutical compositions, methods of using the crystalline salt to treat diseases associated with &bgr;2 adrenergic receptor activity, and processes useful for preparing such crystalline compounds.Type: ApplicationFiled: May 26, 2004Publication date: December 9, 2004Inventors: Ioanna Stergiades, Edward Yost, Cristin Hubbard, Weijiang Zhang
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Patent number: 6814953Abstract: Bronchodilating compositions and methods are provided. The compositions are intended for administration as a nebulized aerosol. In certain embodiments, the compositions contain formoterol, or a derivative thereof. Methods for treatment, prevention, or amelioration of one or more symptoms of bronchoconstrictive disorders using the compositions provided herein are also provided.Type: GrantFiled: May 3, 2002Date of Patent: November 9, 2004Assignee: Dey L.P.Inventors: Partha S. Banerjee, Stephen Pham, Samuel O. Akapo, Imtiaz A. Chaudry
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Publication number: 20040198836Abstract: This invention relates to an improved process for synthesizing (±)-2-Amino-N-[2-(2,5-dimethoxyphenyl]-2-hydroxyethyl acetamide monohydrochloride in good yield and in a cost effective manner from 1-(2,5-dimethoxyphenyl)-2-bromoethanone by reacting the same with hexamine in the presence of novel solvent system comprising Tetrahydrofuran and water. The resulting aminoethanone is acylated with haloacetylchloride and sodium acetate in acetone-water solvent system. This product is reduced selectively first with sodium borohydride and subsequently with stannous chloride. This product is converted in situ to the corresponding hydrochloride salt immediately after reduction on its own.Type: ApplicationFiled: February 6, 2004Publication date: October 7, 2004Inventors: Rajaram Sankara Subramanian, Venkatanathan Satogopan, Rajagopalam Srinivasan
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Publication number: 20040198704Abstract: Novel formulations combining an antiparasitic compounds, such as an avermectin, with a fluorinated chloramphenicol or thiamphenicol derivative antibiotic such as Florfenicol are disclosed. Methods for using such formulations in the treatment and prevention of infectious diseases of bovines and swine, including bovine respiratory disease and parasitic infections are also disclosed.Type: ApplicationFiled: April 2, 2004Publication date: October 7, 2004Applicant: Schering CorporationInventors: Dale E. Shuster, David G. Sawutz, Kanwal J. Varma
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Publication number: 20040180081Abstract: The invention provides compositions, methods and kits for the removal of harmful or irritating substances from bodily surfaces. Kits may include a composition containing capsaicin and a capsaicin-cleansing composition, e.g., a composition in which capsaicin is soluble.Type: ApplicationFiled: March 26, 2004Publication date: September 16, 2004Inventors: Arturo J. Angel, Larry W. Litle, Keith R. Bley, Allan L. Wilcox, Gene Curtis Jamieson, Naweed Muhammad
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Publication number: 20040161481Abstract: Disclosed in certain embodiments is a method for relieving pain at a site in a human or animal in need thereof, comprising administering by injection or infiltration, a dose of a capsaicinoid and coadministering an effective amount of a NSAID to decrease an undesired effect of the capsaicinoid.Type: ApplicationFiled: December 18, 2003Publication date: August 19, 2004Applicant: AlgoRxInventors: Ronald M. Burch, Richard B. Carter, Jeff Lazar
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Publication number: 20040146590Abstract: The present invention provides methods and kits for the selective ablation of pain-sensing neurons. The methods comprise administration of a vanilloid receptor agonist to a ganglion in an amount that causes death of vanilloid receptor-bearing neurons. Accordingly, the present invention provides methods of controlling pain and inflammatory disorders that involve activation of vanilloid receptor-bearing neurons.Type: ApplicationFiled: March 18, 2004Publication date: July 29, 2004Inventors: Michael J Iadarola, Zoltan Olah, Laszlo Karal
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Publication number: 20040122106Abstract: The present invention provides an intraorally rapidly disintegrable tablet which rapidly disintegrates in the oral cavity without water and has a practical hardness, which comprises (a) a pharmacologically active ingredient with a water solubility of at least 1 mg/ml, (b) D-mannitol in the form of crystals or fine particles with primary particle average diameter of at least 30 &mgr;m and a specific surface area of 0.4 m2/g or less, and (c) crospovidone.Type: ApplicationFiled: November 18, 2003Publication date: June 24, 2004Inventors: Motohiro Ohta, Muneko Kuboyama, Hirokazu Yoshimoto, Yasushi Watanabe, Kiyoshi Morimoto, Makoto Kosugi
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Publication number: 20040092600Abstract: A inhibitor of sphingolipids synthesis comprising a compound represented by general formula A. Desirably, a novel inhibitor of sphingolipids synthesis comprising (1R, 3R) N-(3-hydroxy-1-hydroxymethyl-3-phenylpropyl) alkaneamide, wherein carbon number of alkanoyl group is 8-16.Type: ApplicationFiled: September 23, 2003Publication date: May 13, 2004Inventors: Shu Kobayashi, Kentaro Hanada
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Patent number: 6720453Abstract: A method of preparation of a highly pure salt of R,R-formoterol L-tartrate is disclosed. The process provides the most thermodynamically stable polymorph by recrystallization of a novel polymorph.Type: GrantFiled: September 10, 2002Date of Patent: April 13, 2004Assignee: Sepracor Inc.Inventors: Gerald J. Tanoury, Chris H. Senanayake, Donald W Kessler
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Patent number: 6716414Abstract: An aerosol solution composition for use in an aerosol inhaler comprises an active material, a propellant containing a hydrofluoroalkane, a cosolvent and optionally a low volatility component to increase the mass median aerodynamic diameter (MMAD) of the aerosol particles on actuation of the inhaler. The composition is stabilized by using a small amount of mineral acid and a suitable can having part or all of its internal metallic surfaces made of stainless steel, anodized aluminium or lined with an inert organic coating.Type: GrantFiled: May 21, 2001Date of Patent: April 6, 2004Assignee: Chiesi Farmaceutici S.p.A.Inventors: David Lewis, David Ganderton, Brian Meakin, Gaetano Brambilla, Alessandra Ferraris
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Publication number: 20040059001Abstract: The present invention relates to an extended release pharmaceutical composition containing metformin and a rate controlling polymer and a process for the preparation thereof.Type: ApplicationFiled: September 18, 2003Publication date: March 25, 2004Inventors: Deepak Murpani, Ashish Madan, Vinod Kumar Arora, Rajiv Malik
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Publication number: 20040006102Abstract: The invention provides novel &bgr;2 adrenergic receptor agonist compounds. The invention also provides pharmaceutical compositions comprising such compounds, methods of using such compounds to treat diseases associated with &bgr;2 adrenergic receptor activity, and processes and intermediates useful for preparing such compounds.Type: ApplicationFiled: May 27, 2003Publication date: January 8, 2004Inventors: Edmund J. Moran, Eric Fournier
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Publication number: 20040006135Abstract: The present invention relates to a method of treating depression or anxiety in a mammal, including a human, by administering to the mammal a CNS-penetrant NK-1 receptor antagonist (e.g., a substance P receptor antagonist) in combination with an NK-3 antagonist agent. It also relates to pharmaceutical compositions containing a pharmaceutically acceptable carrier, a CNS-penetrant NK-1 receptor antagonist and an NK-3 antagonist.Type: ApplicationFiled: March 12, 2003Publication date: January 8, 2004Applicant: Pfizer Inc.Inventors: Susan B. Sobolov-Jaynes, John A. Lowe, Stafford McLean
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Publication number: 20040001895Abstract: The present invention relates to a method of treating depression or anxiety in a mammal, including a human, by administering to the mammal a CNS-penetrant NK-1 receptor antagonist (e.g., a substance P receptor antagonist) in combination with a PDE IV inhibitor. It also relates to pharmaceutical compositions containing a pharmaceutically acceptable carrier, a CNS-penetrant NK-1 receptor antagonist and a PDE IV inhibitor.Type: ApplicationFiled: March 13, 2003Publication date: January 1, 2004Applicant: Pfizer Inc.Inventors: Susan B. Sobolov-Jaynes, Christopher J. Schmidt, Lorraine A. Lebel
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Publication number: 20030236238Abstract: The invention relates to novel pharmaceutical compositions useful in the treatment of respiratory disorders such as asthma, rhinitis and chronic obstructive pulmonary disease (COPD).Type: ApplicationFiled: November 15, 2002Publication date: December 25, 2003Inventors: Eva Trofast, Karin Malmqvist-Granlund, Per-Gunnar Nilsson, Kyrre Thalberg
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Publication number: 20030236234Abstract: This invention relates to novel fluorinated phenyl thiphenyl (also named diarylsulfide) derivatives and their use in Positron Emission Tomagraphy (PET) imaging of Serotonin Transporters (SERTS). The present invention also provides diagnostic compositions comprising the novel compounds of the present invention, and a pharmaceutically acceptable carrier or diluent. The invention further provides a method of imaging SERTS, comprising introducing into a patient a detectable quantity of a labeled compound of the present invetion, or a pharmaceutically acceptable salt, ester, amide or prodrug thereof.Type: ApplicationFiled: March 14, 2003Publication date: December 25, 2003Inventors: Hank F. Kung, Chyng-Yann Shiue, Shunichi Oya, Seok Rye Choi, Grace G. Shiue, Ping Fang
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Publication number: 20030232883Abstract: This invention relates to N-acylamino aryl derivatives of the formula 1Type: ApplicationFiled: May 27, 2003Publication date: December 18, 2003Inventors: Synese Jolidon, Rosa Maria Rodriguez Sarmiento, Andrew William Thomas, Rene Wyler
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Patent number: 6656453Abstract: This invention relates to aerosol formulations of use for the administration of medicaments by inhalation. More particularly, the invention relates to a pharmaceutical aerosol formulation which comprises particulate salbutamol sulphate having a crystalline form in which the outer layer of the crystals is substantially non-amorphous; and 1,1,1,2-tetrafluoroethane. A method of treating respiratory disorders which comprises administration by inhalation of an effective amount of a pharmaceutical aerosol formulation as defined is also described.Type: GrantFiled: June 27, 2002Date of Patent: December 2, 2003Assignee: SmithKline Beecham CorporationInventors: Michael Thomas Riebe, Sarvajna Kumar Dwivedi, Li Li-Bovet
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Publication number: 20030216447Abstract: Novel formulations combining a non-steroidal anti-inflammatory drug (NSAID) such as flunixin, with a fluorinated chloramphenicol or thiamphenicol derivative antibiotic such as florfenicol are disclosed. Methods for using such formulations in the treatment and prevention of infectious diseases of bovines and swine, including bovine respiratory disease and swine respiratory disease, are also disclosed.Type: ApplicationFiled: May 20, 2003Publication date: November 20, 2003Applicant: SCHERING-PLOUGH ANIMAL HEALTHInventors: Raul E. Kohan, Kanwal J. Varma, Robert D. Simmons, Abu Huq
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Patent number: 6642243Abstract: This invention is a safe and effective composition and method for treating acute migraine attacks using pseudoephedrine, acetaminophen, and other agents in an orally administrated form to alleviate the pain and cluster of symptoms characteristic of migraine attacks such as nausea, photophobia, phonophobia, and functional disabilities as well as the prodrome phase of a migraine attack.Type: GrantFiled: June 14, 2000Date of Patent: November 4, 2003Inventor: Ashkan Imanzahrai
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Publication number: 20030203970Abstract: A method and composition are disclosed utilizing the pure (R,R) isomer of formoterol, which is a potent bronchodilator with reduced adverse effects, a low incidence of the development of tolerance and an increased duration of action, as compared to racemic formoterol.Type: ApplicationFiled: June 9, 2003Publication date: October 30, 2003Applicant: Sepracor Inc.Inventors: Gunnar Aberg, John Morley
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Publication number: 20030199473Abstract: This invention concerns the compounds of formula 1Type: ApplicationFiled: March 26, 2003Publication date: October 23, 2003Applicant: Janssen Pharmaceutica N.V.Inventors: Paul A.J. Janssen, Jan Heeres, Henri E.L. Moereels, Michael Joseph Kukla, Donald W. Ludovici
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Patent number: 6617351Abstract: The present invention provides certain amide, carbamate and urea derivatives useful for potentiating glutamate receptor function in a mammal and therefore, useful for treating a wide variety of conditions, such as psychiatric and neurological disorders.Type: GrantFiled: January 23, 2001Date of Patent: September 9, 2003Assignee: Eli Lilly and CompanyInventors: Macklin Brian Arnold, David Michael Bender, Thomas John Bleisch, Winton Dennis Jones, Paul Leslie Ornstein, Hamideh Zarrinmayeh, Dennis Michael Zimmerman
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Patent number: 6602903Abstract: The invention relates to compounds of formula (I): and medicinal products containing the same are useful in treating or in preventing melatoninergic disorders.Type: GrantFiled: August 28, 2001Date of Patent: August 5, 2003Assignee: Les Laboratories ServierInventors: Gérald Guillaumet, Marie-Claude Viaud, Ahmed Mamai, Isabelle Charton, Pierre Renard, Caroline Bennejean, Béatrice Guardiola, Philippe Daubos
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Publication number: 20030133880Abstract: Powdery pharmaceutical compositions including an active ingredient and carrier particles containing only a small amount of lubricant, 0.05-0.5% by weight, are used to prepare dry powder inhalers in order to increase the fine particle dose. A process for coating the surface of the carrier particles with such little amount of lubricant is also provided. Use of limited amount of lubricant is safe and provides ordered stable mixtures without segregation of the active particles during handling and before use.Type: ApplicationFiled: February 5, 2003Publication date: July 17, 2003Applicant: Chiesi Farmaceutici S.p.A.Inventors: Rossella Musa, Paolo Ventura, Paolo Chiesi
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Patent number: 6583319Abstract: The invention relates to compounds of for a (I): wherein: R represents ORa, SRa or Ra or a cyclic group A is a cyclic structure G1 and G2 represent an alkylene chain or a single bond B represents —NR1aC(Q)R2a, —NR1aC(Q)NR2aR3a or C(Q)NR1aR2a p and q are such that 1≦p+q≦4, and medicinal products containing the same which are useful in treating or in preventing melatoninergic disorders.Type: GrantFiled: October 12, 1999Date of Patent: June 24, 2003Assignee: Les Laboratoires ServierInventors: Michel Langlois, Monique Mathe-Allainmat, Marie Lefas-Le Gall, Caroline Bennejean, Pierre Renard, Philippe Delagrange
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Publication number: 20030109510Abstract: The present invention is concerned with pharmaceutical formulations comprising a combination of (R,R)-formoterol and budesonide and the use of such formulations in medicine, particularly in the prophylaxis and treatment of respiratory diseases.Type: ApplicationFiled: October 15, 2002Publication date: June 12, 2003Inventor: Brian Charles Gavin
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Publication number: 20030100614Abstract: Use of thiamphenicol and derivatives thereof for the preparation of pharmaceutical compositions useful for the treatment Chlamydia pneumoniae infections is described.Type: ApplicationFiled: December 11, 2001Publication date: May 29, 2003Inventors: Giovanni Battista Colombo, Domenico Ungheri, Luciano Licciardello, Maria Rita Gismondo, Lorenzo Drago
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Patent number: 6555710Abstract: The present invention relates to compounds of formula (I) wherein R1 and R2 independently represent one or more, same or different substituents selected from the group consisting of halogen, hydroxy, mercapto, trifluoromethyl, amino (C1-C3)alkyl, (C2-C3)olefinic group, (C1-C3)alkoxy, (C1-C3)alkylthio, (C1-C6)alkylamino, (C1-C3)alkoxycarbonyl, cyano, carbamoyl, phenyl, or nitro; R2 further being represented by hydrogen; R3 represents hydrogen, halogen, hydroxy, mercapto, trifluoromethyl, amino, (C1-C3)alkyl, (C2-C3)olefinic group, (C1-C3)alkoxy, (C1-C3)alkylthio, (C1-C6)alkylamino, (C1-C3)alkoxycarbonyl, phenyl, cyano, carboxy or carbomoyl; R4 represents hydrogen, (C1-C3)alkyl, or allyl; X represents oxygen or sulpher; with the proviso that formula (I) does not comprise the compound 2,2,2-trifluoro-N-[2-[3-chloro-4-(2-methylbenzoyl)-phenylamino]-phenyl]acetamide wherein R1 is a 2-methyl, R2 is 2-chloro, R3 and R4 is hydrogen, and X is oxygen; and a salt thereof with a pharmaceutically accepType: GrantFiled: March 15, 2002Date of Patent: April 29, 2003Assignee: Leo Pharmaceutical Products Ltd a/s Lovens Kemiske Fabrik ProduktionsaktieselskabInventor: Erik Rytter Ottosen
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Publication number: 20030078269Abstract: The invention describes formulations that include either metformin, sulfonylurea or a biguanide-sulfonylurea combination as one active ingredient in addition to specific, other active ingredients. The compositions and dosage forms of the invention are clinically useful as methods for increasing the effectiveness, efficiency and safety of the included biguanide (metformin) and/or sulfonylurea in the prevention and treatment of insulin resistance and diabetes mellitus. The carefully chosen additional active ingredients of the invention are designed in a modular fashion to prevent and rectify adverse events associated with insulin resistance syndrome and diabetes mellitus, and those adverse incidences associated with the concurrent use of metformin and/or the sulfonylureas. When clinically administered, the invention will provide therapeutic levels of metformin and of a sulfonylurea, alone or in combination, and broaden their usefulness.Type: ApplicationFiled: March 7, 2002Publication date: April 24, 2003Applicant: ChronoRX, LLCInventors: Don C. Pearson, Kenneth T. Richardson
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Publication number: 20030073685Abstract: There is disclosed the use of a compound of formula (I), wherein R1, R2, X, Y, V, W and Z are as defined in the specification, and pharmaceutically acceptable salts, enantiomers or racemates thereof, in the manufacture of a medicament, for the treatment or prophylaxis of diseases or conditions in which inhibition of nitric oxide synthase activity is beneficial. Certain novel compounds of formula (Ia) and pharmaceutically acceptable salts thereof, and enantiomers and racemates thereof are disclosed; together with processes for their preparation, compositions containing them and their use in therapy. The compounds of formulae (I) and (Ia) are inhibitors of the enzyme nitric oxide synthase and are thereby particularly useful in the treatment or prohylaxis of inflammatory disease.Type: ApplicationFiled: August 22, 2002Publication date: April 17, 2003Inventors: David Cheshire, Stephen Connolly, David Cox, Ian Millichip
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Patent number: 6537524Abstract: A medicament containing, separately or together, (A) formoterol or a pharmaceutically acceptable salt thereof or a solvate of formoterol or said salt and (B) a tiotropium salt of a pharmaceutically acceptable acid, for simultaneous, sequential or separate administration in the treatment of an inflammatory or obstructive airways disease.Type: GrantFiled: August 8, 2001Date of Patent: March 25, 2003Assignee: Novartis AGInventors: Ian Francis Hassan, Jeremy Guy Clarke, Bernard Cuenoud
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2-aminopropane-1,3-diol compounds, medicinal use thereof, and intermediates in synthesizing the same
Patent number: RE39072Abstract: The present invention relates to a compound of the general formula wherein R1, R2, R3 and R4 are each a hydrogen or an acyl, a pharmaceutically acceptable acid addition salt thereof or a hydrate thereof; a pharmaceutical comprising this compound; a pharmaceutical composition comprising this compound and a pharmaceutically acceptable carrier; and 2-amino-2-(2-(4-(1-hydroxy-5-phenylpentyl)phenyl)ethyl)propane-1,3-diol or 2-amino-2-(2-(4-formylphenyl)ethyl)propane-1,3-diol, the derivatives of the two compounds whose amino group and/or hydroxy group are(is) protected or a salt thereof. The compound of the present invention shows superior immunosuppressive action with less toxicity and higher safety, and is useful as a drug for prevention or suppression of rejection of organs or bone marrow transplantation, or as a drug for prevention or treatment of various autoimmune diseases or allergic diseases.Type: GrantFiled: April 3, 1998Date of Patent: April 18, 2006Assignee: Mitsubishi Pharma CorporationInventors: Kunitomo Adachi, Yoshiyuki Aoki, Tokushi Hanano, Koji Teshima, Yukio Hoshino, Tetsuro Fujita