One Of The Cyclos Is A 1,2-thiazine (e.g.,1,2-benzothiazines, Etc.) Patents (Class 514/226.5)
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Patent number: 6894041Abstract: This application is directed to compounds useful as inhibitors of PDE4 in the treatment of diseases regulated by the activation and degranulation of eosinophils, especially asthma, chronic bronchitis, and chronic obstructuive pulmonary disease, of the formula: where Y is ?C(R1a)— or —[N(O)k]— where k is 0 or 1; G1 is a saturated or unsaturated carbon ring system that is a 3- to 7-membered monocyclic, or that is a 7- to 12-membered, fused polycyclic; provided that G1 is not a discontinuous or restricted biaryl moiety as defined under G2; where optionally one carbon atom may be replaced by a heteroatom selected from N, O, and S; where optionally a second carbon atom thereof, and further optionally a third carbon atom thereof may be replaced by N; —G2 is a saturated or unsaturated carbon ring system that is a 3- to 7-membered monocyclic; or that is a 7- to 12-membered, fused polycyclic; or that is a 7- to 18-membered discontinuous or restricted biaryl moiety; wherein for each of the carbon ring systems recitType: GrantFiled: November 20, 2002Date of Patent: May 17, 2005Assignee: Pfizer IncInventors: Anthony Marfat, Michael William McKechney
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Patent number: 6869945Abstract: This application is directed to compounds useful as inhibitors of PDE4 in the treatment of diseases regulated by the activation and degranulation of eosinophils, especially asthma, chronic bronchitis, and chronic obstructuive pulmonary disease, of the formula: where Y is ?C(R1a)— or —[N?(O)k]— where k is 0 or 1; G1 is a saturated or unsaturated carbon ring system that is a 3- to 7-membered monocyclic, or that is a 7- to 12-membered, fused polycyclic; provided that G1 is not a discontinuous or restricted biaryl moiety as defined under G2; where optionally one carbon atom may be replaced by a heteroatom selected from N, O, and S; where optionally a second carbon atom thereof, and further optionally a third carbon atom thereof may be replaced by N; -G2 is a saturated or unsaturated carbon ring system that is a 3- to 7-membered monocyclic; or that is a 7- to 12-membered, fused polycyclic; or that is a 7- to 18-membered discontinuous or restricted biaryl moiety; wherein for each of the carbon ring systems reType: GrantFiled: November 20, 2002Date of Patent: March 22, 2005Assignee: Pfizer IncInventors: Anthony Marfat, Michael William McKechney
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Patent number: 6869948Abstract: The invention relates in its first aspect to a rapidly decomposing tablet for pain therapy containing meloxicam [4-hydroxy-2-methyl-N-(5-methyl-2-thiazolyl)-2H-1,2-benzothiazine-3-carboxamide-1,1-dioxide] in the form of a salt with an inorganic or organic base providing rapid absorption of the active substance, the process of its preparation by direct tabletting, and furthermore relates in a second aspect to the crystalline meloxicam meglumin salt mono- and dihydrate and the preparation thereof.Type: GrantFiled: March 26, 1999Date of Patent: March 22, 2005Assignee: Boehringer Ingelheim Pharma KGInventors: Thomas Bock, Paul Saegmueller, Peter Sieger, Dietrich Tuerck
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Patent number: 6867236Abstract: The present invention relates, in general, to a method of preventing or delaying the onset of Alzheimer's disease and related neurodegenerative disorders. The invention also relates to a method of treating Alzheimer's disease and related neurodegenerative disorders so as to ameliorate the further progress of symptoms. The methods involve the administration of a non-steroidal anti-inflammatory agent and/or a histamine H2 receptor blocking agent. According to indication, the present method can be applied to individuals who are currently asymptomatic but at risk of developing Alzheimer's disease, to individuals who have mild cognitive symptoms that may either denote an incipient prodrome of Alzheimer's disease or represent early symptoms (prodromal stage), or to individuals who have a clinical diagnosis of Alzheimer's disease.Type: GrantFiled: April 28, 1999Date of Patent: March 15, 2005Assignee: Duke UniversityInventors: John C. S. Breitner, Kathleen A. Welsh-Bohmer
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Patent number: 6844338Abstract: A pharmaceutical compound of the formula (I) in which R1 and R2 are each hydrogen or C1-6 alkyl, R3 is —SR10, —SOR10, —SO2R10, —COR10, —CH2OH or —CONHR11, where R10 is C1-6 alkyl and R11 is hydrogen or C1-6 alkyl, R4, R5, R6 and R7 are each hydrogen or C1-6alkyl, provided that at least one of R4, R5, R6 and R7 is C1-6alkyl, R8 and R9 are each hydrogen, halo, C1-6 alkyl or cyano, n is 0 or 1 and m is 2 or 3, x is a (a) or (b), and y is (c) or (d), wherein R12 and R13 are each hydrogen, C1- alkyl, cyclopropyl or cyclopropyl-C1-6 alkyl; and salts thereof.Type: GrantFiled: May 4, 2001Date of Patent: January 18, 2005Assignee: Eli Lilly and CompanyInventors: John Fairhurst, Peter Gallagher
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Publication number: 20040242571Abstract: This invention relates to novel benzothiazine derivatives of Formula I useful as modulators of the AMPA sensitive glutamate receptors, pharmaceutical compositions comprising such compounds and their use in therapy.Type: ApplicationFiled: March 15, 2004Publication date: December 2, 2004Inventors: Alex Haahr Gouliaev, Morgens Larsen, Thomas Varming, Claus Mathiesen, Tina Holm Johansen, Karin Sandager Nielsen, Barbara Hartz, Jorgen Scheel-Kruger
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Publication number: 20040234596Abstract: The present invention relates to a fast disintegrating tablet comprising meloxicam or a pharmaceutically acceptable salt thereof, starch or various starches, glidant and at least one additional excipient.Type: ApplicationFiled: June 28, 2004Publication date: November 25, 2004Applicant: Boehringer Ingelheim International GmbHInventors: Toshimitsu Ohki, Wakuko Yamaguchi, Kotoe Ohta
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Patent number: 6811768Abstract: A method for lessening or preventing non-pulmonary ischemia-reperfusion injury or inflammation in a mammal by identifying a mammal which has ischemia-reperfusion or is at risk for developing ischemia-reperfusion in a non-pulmonary tissue; and causing the mammal to inhale a therapeutically effective amount of gaseous nitric oxide sufficient to diminish the ability of leukocytes or platelets to become activated in a manner that contributes to an inflammatory process at the site of the ischemia-reperfusion or inflammation in the non-pulmonary tissue, thereby lessening or preventing non-pulmonary ischemia-reperfusion injury in the mammal.Type: GrantFiled: October 27, 2003Date of Patent: November 2, 2004Assignee: The General Hospital CorporationInventors: Warren M. Zapol, Kenneth D. Bloch, Anthony Rosenzweig
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Publication number: 20040204413Abstract: The present invention provides a pharmaceutical composition and dosage form containing in combination a COX-II inhibitor and a muscle relaxant. The pharmaceutical composition is useful for the treatment of pain and pain related disorders and symptoms. The combination provides an improved therapeutic response as compared to either drug alone. The pharmaceutical composition can be included in any dosage form.Type: ApplicationFiled: January 26, 2001Publication date: October 14, 2004Inventors: Joaquina Faour, Juan A. Vergez
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Publication number: 20040180092Abstract: Water soluble meloxicam granules comprising:Type: ApplicationFiled: October 27, 2003Publication date: September 16, 2004Applicant: Boehringer Ingelheim Vetmedica GmbHInventors: Stefan Henke, Martin Andreas Folger, Jens Schmalz, Diana Christine Keilhofer, Hans-Juergen Kroff, Nina Herz
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Publication number: 20040176355Abstract: The present invention discloses compounds which are novel antagonists for melanin-concentrating hormone (MCH), as well as methods for preparing such compounds. In other aspects, the invention is directed to pharmaceutical compositions comprising such MCH antagonists as well as methods of using them to treat obesity, metabolic disorders, eating disorders such as hyperphagia, and diabetes.Type: ApplicationFiled: February 26, 2004Publication date: September 9, 2004Applicant: Schering CorporationInventors: Thavalakulamgara K. Sasikumar, Wen-Lian Wu, Duane A. Burnett, Li Qiang
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Publication number: 20040171611Abstract: The present invention relates to a new crystalline modification of the compound 4-hydroxy-2-methyl-N-(5-methyl-2-thiazolyl)-2H-1,2-benzothiazin-3-carboxamide-1,1-dioxide in the form of an acetic acid solvate of formula I as well as the use thereof as a pharmaceutical composition.Type: ApplicationFiled: September 22, 2003Publication date: September 2, 2004Applicant: Boehringer Ingelheim Pharma GmbH & Co. KGInventors: Guenter Trummlitz, Rainer Soyka, Peter Sieger, Ulrike Werthmann, Peter Luger
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Patent number: 6759406Abstract: Compounds of formula corresponding to either formula (Ia) or (Ib): wherein: M represents a molecule that can be used for the treatment or diagnosis of pathologies caused by attack on the cartilage, R1, R2 and R3 represent an alkyl group, or R1, R2 and R3, together with the nitrogen atom carrying them, form a heterocycle, X represents a (C1-C6)alkylene chain in which one or more —CH2— groups are optionally replaced by a sulphur atom, an oxygen atom, or an —NR—, —CO—, —CO—NH—, —CO2—, —SO— or —SO2— group, n represents 0 or 1, Hal represents a halogen atom, or, R4 represents an alkyl group, Hal represents a halogen atom, represents a molecule that can be used for the treatment or diagnosis of pathologies caused by attack on the cartilage, wherein the nitrogen atom may optionally be included in a saturated or unsaturated nitrogen-containing heterocyclic system, or iType: GrantFiled: March 25, 2002Date of Patent: July 6, 2004Assignees: Les Laboratoires Servier, INSERMInventors: Jean-Claude Madelmont, Isabelle Giraud, Colette Nicolas, Jean-Claude Maurizis, Maryse Rapp, Monique Ollier, Pierre Renard, Daniel-Henri Caignard
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Publication number: 20040127705Abstract: A pyrrolesulfonamide derivative having the following formula (I): 1Type: ApplicationFiled: July 10, 2003Publication date: July 1, 2004Applicant: DAIICHI PHARMACEUTICAL CO., LTD.Inventors: Akira Mizuno, Makoto Shibata, Tomoe Kamei, Harukazu Fukami, Norio Inomata
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Patent number: 6756370Abstract: The invention relates to compounds of formula (I), wherein R1, R2 and A have the meanings given in claim 1, are potent 5-HT2A antagonists and are suitable for treating psychoses, schizophrenia, depression, neurological disorders, impaired memory, Parkinson's disease, amyotrophic lateral sclerosis, Alzheimer's disease, Huntington's disease, eating disorders such as bulimia and anorexia nervosa, Pre-Menstrual Syndrome and/or for positively influencing obsessive-compulsive disorders, (OCD).Type: GrantFiled: February 21, 2002Date of Patent: June 29, 2004Assignee: Merck Patent GmbHInventors: Helmut Prücher, Henning Böttcher, Karl-August Ackermann, Rudolf Gottschlich, Christoph van Amsterdam, Christoph Seyfried, Jürgen Harting, Gerd Bartoszyk, Hartmut Greiner
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Publication number: 20040116413Abstract: The present invention provides compounds of formula I useful as antimicrobial agents 1Type: ApplicationFiled: November 14, 2001Publication date: June 17, 2004Inventors: Michael J. Genin, Michael Robert Barbachyn, Jackson B. Hester, Paul D. Johnson, Fred L. Ciske
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Publication number: 20040110747Abstract: The invention relates to a method of treatment or prevention of acute coronary syndrome or related conditions or reducing the risk of cardiovascular events comprising the administration of a therapeutically or prophylactically effective amount of meloxicam in combination with a therapeutically or prophylactically effective amount of an antiplatelet agent to a patient in need of such treatment. The invention also provides pharmaceutical compositions comprising meloxicam and an antiplatelet agent as a combined preparation suitable for use in these indications. Furthermore, the invention provides the use of meloxicam for manufacture of a pharmaceutical composition for treatment or prevention of acute coronary syndrome and related conditions when used in combination with an antiplatelet agent.Type: ApplicationFiled: December 10, 2002Publication date: June 10, 2004Applicant: Boehringer Ingelheim International GmbHInventor: Raul Altman
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Publication number: 20040063697Abstract: The present invention provides compositions and methods for the treatment or prevention of a vaso-occlusive event. More particularly, the invention provides a combination therapy for the treatment or prevention of a vaso-occlusive event comprising the administration to a subject of a thrombolytic agent in combination with a cyclooxygenase-2 selective inhibitor.Type: ApplicationFiled: June 30, 2003Publication date: April 1, 2004Inventor: Peter C. Isakson
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Publication number: 20040063696Abstract: 1 wherein: represents a single or double bond, R1 represents a hydrogen atom or a hydroxy, alkoxy, acyloxy, alkylsulphonyloxy, arylsulphonyloxy or arylalkoxy group, R2 represents a hydrogen atom or an alkyl group, R3 and R4, which may be identical or different, each represent a hydrogen atom, a halogen atom or an alkyl, hydroxy or alkoxy group, Ak represents an alkylene chain, R5, R6 and R7, which may be identical or different, each represent an alkyl group, or R5, R6 and R7, taken together with the nitrogen atom carrying them, form a saturated or unsaturated nitrogen-containing heterocycle,Type: ApplicationFiled: June 20, 2003Publication date: April 1, 2004Inventors: Jean-Claude Madelmont, Isabelle Giraud, Aurelien Vidal, Emmanuelle Mounetou, Maryse Rapp, Jean-Claude Maurizis, Pierre Renard, Daniel-Henri Caignard, Jean-Guy Bizot-Espiard
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Patent number: 6713463Abstract: A method of reducing or inhibiting mucositis in a patient, which includes administering an inflammatory cytokine inhibitor or a mast cell inhibitor, or a combination thereof, is disclosed.Type: GrantFiled: September 27, 2002Date of Patent: March 30, 2004Assignee: Mucosal Therapeutics, LLCInventors: Stephen T. Sonis, Edward G. Fey
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Publication number: 20040043992Abstract: A method for alleviating organ injury during organ operation or transplantation associated with vascular occlusion to a patient in need thereof comprising administering to the patient an effective amount of meloxicam or a pharmacologically acceptable salt thereof.Type: ApplicationFiled: May 21, 2003Publication date: March 4, 2004Applicant: Boehringer Ingelheim International GmbHInventors: Rene H. Tolba, Yuzo Yamamoto
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Patent number: 6682747Abstract: The present invention relates to orally administered suspensions of pharmaceutical active substances of the NSAID type, particularly the antirheumatic agent Meloxicam, which are stabilized by the addition of small amounts of highly dispersed silicon dioxide using high shear forces and adding small amounts of hydrophilic polymers to form a three-dimensional siloid structure, and a process for the preparation thereof.Type: GrantFiled: November 7, 2000Date of Patent: January 27, 2004Assignee: Boehringer Ingelheim Pharma KGInventors: Dietrich Türck, Veit Schmelmer
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Publication number: 20030236252Abstract: Described are bicycle-substituted cyclohexylamines of Formula (I) and their pharmaceutically acceptable salts thereof. The compounds are antagonists of NMDA receptor channel complexes useful for treating cerebral vascular disorders such as, for example, cerebral ischemia, cardiac arrest, stroke, and Parkinson's specification. disease. The substituents are defined in the specification.Type: ApplicationFiled: November 12, 2002Publication date: December 25, 2003Inventors: Sham Shridhar Nikam, Ian Leslie Scott, Brian Alan Sherer, Lawrence David Wise
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Patent number: 6667056Abstract: A pharmaceutical formulation in the form of a fast dissolving tablet comprising an active ingredient, sodium glycine carbonate and an acid capable of reacting rapidly with sodium glycine carbonate to release carbon dioxide.Type: GrantFiled: August 20, 2001Date of Patent: December 23, 2003Assignee: Chiesi Farmaceutici S.p.A.Inventors: Paolo Chiesi, Paolo Ventura, Rosa Mezzadri, Gaetano Brambilla, Daniela Acerbi
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Publication number: 20030232810Abstract: Described are heterocycle-substituted cyclohexylamines of formula (I), and their pharmaceutically acceptable salts thereof. The compounds of formula (I) are antagonists of NMDA receptor channel complexes useful for treating cerebral vascular disorders such as, for example, cerebral ischemia, cardiac arrest, stroke, and Parkinson's disease.Type: ApplicationFiled: December 3, 2002Publication date: December 18, 2003Inventors: Russell Joseph Deorazio, Sham Shridhar Nikam, Ian Leslie Scott, Brian Alan Sherer, Lawrence David Wise
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Publication number: 20030232787Abstract: The present invention is a novel combination effective for alleviating pain comprising a pain alleviating effective amount of an endothelin receptor antagonist or a pharmaceutically acceptable salt thereof and from 1 to 3 compounds independently selected from the group consisting of antiepileptic compounds having pain alleviating properties and analgesics, and pharmaceutically acceptable salts thereof, and pharmaceutical compositions comprising same. The administration of endothelin receptor antagonists in these novel combinations results in an improved reduction in the frequency and severity of pain. The incidence of unwanted side effects can be reduced by these novel combinations in comparison to using higher doses of a single agent treatment to achieve a similar therapeutic effect. The present invention is also directed to methods of using effective amounts of the novel combinations and pharmaceutical compositions thereof to treat pain in mammals, including a human.Type: ApplicationFiled: November 26, 2002Publication date: December 18, 2003Inventor: David James Dooley
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Patent number: 6664251Abstract: Disclosed are benzothiazine derivatives represented by the following formula (I): wherein the dashed line indicates the presence or absence of a bond; Z represents one of the following groups: in which R1 and R2 individually represent alkyl, aralkyl or the like, R3 represents H, alkyl or the like, R4 represents H, aralkyl or the like, X1, X2 and X3 individually represent O or S, and G represents substituted or unsubstituted ethylene, trimethylene or the like; Q1 and Q2 individually represent H, OH, halogen, alkoxy or the like; A represents alkylene, alkenylene or the like; Y represents CH, C═ or N; when Y is CH, m stands for 0 or 1, n stands for 1 or 2, B represents O, S, carbonyl or the like, when Y is C═, m stands for 1, n stands for 1 or 2, B represents: in which the double bond is linked to Y, R6 represents substituted or unsubstituted aryl or the like; when Y is N, m stands for 0 or 1, n stands for 2 or 3 and B represents carbonyl, sulfonylType: GrantFiled: September 19, 2001Date of Patent: December 16, 2003Assignee: Daiichi Suntory Pharma Co., Ltd.Inventors: Akira Mizuno, Makoto Shibata, Tomoe Iwamori, Norio Inomata
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Patent number: 6656452Abstract: A method for lessening or preventing non-pulmonary ischemia-reperfusion injury or inflammation in a mammal by identifying a mammal which has ischemia-reperfusion or is at risk for developing ischemia-reperfusion in a non-pulmonary tissue; and causing the mammal to inhale a therapeutically effective amount of gaseous nitric oxide sufficient to diminish the ability of leukocytes or platelets to become activated in a manner that contributes to an inflammatory process at the site of the ischemia-reperfusion or inflammation in the non-pulmonary tissue, thereby lessening or preventing non-pulmonary ischemia-reperfusion injury in the mammal.Type: GrantFiled: November 14, 1997Date of Patent: December 2, 2003Assignee: The General Hospital CorporationInventors: Warren M. Zapol, Kenneth D. Bloch
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Publication number: 20030211163Abstract: The invention provides combination therapies for treating papilloma virus.Type: ApplicationFiled: January 10, 2003Publication date: November 13, 2003Inventor: Kong Teck Chong
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Publication number: 20030186973Abstract: The present invention provides 2-thia-1,6,8-triaza-naphthalene-2,2-dioxide inhibitors of cyclin-dependent kinases, uses thereof and pharmaceutical compositions thereof.Type: ApplicationFiled: January 21, 2003Publication date: October 2, 2003Inventor: Joseph Thomas Repine
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Patent number: 6620853Abstract: Methods and compositions for the prevention and/or treatment of vascular restenosis, the methods comprising administering to individuals in need thereof, an effective amount of a non-steroidal anti-inflammatory drug alone or in combination with other conventional therapies to induce apoptosis, reduce proliferation, induce quiescence, inhibit cell migration, or influence cell differentiation of the cells in the vascular wall and or/induce hypolipidemia.Type: GrantFiled: December 8, 1999Date of Patent: September 16, 2003Assignees: Mount Sinai School of Medicine, The Rockefeller UniversityInventors: Steven Shiff, Edward A. Fisher, Hayes M. Dansky, Ernane Reis
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Patent number: 6605627Abstract: In accordance with the present invention, there is provided a class of compounds which are capable of modulating processes mediated by peroxisome proliferator activated receptor-gamma (PPAR-&ggr;). The identification of such compounds makes it possible to intervene in PPAR-&ggr; mediated pathways.Type: GrantFiled: May 8, 2002Date of Patent: August 12, 2003Assignee: The Salk Insitute for Biological StudiesInventors: Ronald M. Evans, Barry M. Forman
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Publication number: 20030119825Abstract: Aqueous cyclodextrin-free solution of meloxicam suitable for administration by needleless injection, containing a pharmacologically acceptable meloxicam salt of an organic or inorganic base and one or more suitable excipients, the content of dissolved meloxicam salt being from 35 to 100 mg/ml. The formulation according to the invention has a shelf-life of up to 24 months or more.Type: ApplicationFiled: December 9, 2002Publication date: June 26, 2003Applicant: Boehringer Ingelheim Vetmedica GmbHInventors: Martin Andreas Folger, Stefan Henke, Bernhard Hassel, Bernd Zierenberg
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Publication number: 20030109520Abstract: Nonsteroidal antiinflammatory drugs which have been substituted with a nitrogen monoxide group; compositions comprising (i) a nonsteroidal antiinflammatory drug, which can optionally be substituted with a nitrogen monoxide group and (ii) a compound that directly donates, transfers or releases a nitrogen monoxide group (preferably as a charged species, particularly nitrosonium); and methods of treatment of inflammation, pain, gastrointestinal lesions and/or fever using the compositions are disclosed. The compounds and compositions protect against the gastrointestinal, renal and other toxicities that are otherwise induced by nonsteroidal antiinflammatory drugs.Type: ApplicationFiled: October 22, 2002Publication date: June 12, 2003Inventors: David S. Garvey, L. Gordon Letts, H. Burt Renfroe, Sang William Tam
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Patent number: 6562811Abstract: Pyridine compounds of general formula: wherein —R1 represents in which R11 is hydrogen, C1-6 alkyl, halogen, hydroxy, C1-12 alkoxy, nitro, amino, C1-6 alkylsulfonylamino, C1-6 alkoxycarbonyl, C1-6 alkylamino, di(C1-6 alkyl)amino, C1-6 alkanoylamino, phenyl C1-6 alkylamino, phenylsulfonylamino, or —O—(CH2)n—R111; R2 represents hydrogen or halogen; R3 represents hydrogen, —CR31R32R33, or —NR34R35; R4 is hydrogen, carbamoyl, CN, carboxyl, etc.; R5 is amino, C1-6 alkylamino, di C1-6 alkylamino, etc. or salt thereof. The compound has an excellent anti-inflammatory activity, and other biological activity.Type: GrantFiled: September 18, 2001Date of Patent: May 13, 2003Assignee: Bayer AktiengesellschaftInventors: Toshiki Murata, Masaomi Umeda, Sachiko Sakakibara, Takashi Yoshino, Hiroki Sato, Tsutomu Masuda, Yuji Koriyama, Mitsuyuki Shimada, Takuya Shintani, Hiroshi Kadono, Timothy B. Lowinger, Karl B. Ziegelbauer, Kinji Fuchikami, Hiroshi Komura
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Publication number: 20030078256Abstract: Disclosed are benzothiazine derivatives represented by the following formula (I): 1Type: ApplicationFiled: September 19, 2001Publication date: April 24, 2003Applicant: SUNTORY LIMITEDInventors: Akira Mizuno, Makoto Shibata, Tomoe Iwamori, Norio Inomata
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Publication number: 20030073684Abstract: The instant invention is a series of benzothiazine dioxides, or a pharmaceutically acceptable salt thereof, which are potent endothelin A antagonists with profound in vitro activity, and improved syntheses for the Formula 1 1Type: ApplicationFiled: June 3, 2002Publication date: April 17, 2003Inventors: Amy Mae Bunker, Xue-Min Cheng, Annette Marian Doherty, Jeremy John Edmunds, Gerald David Kanter, Chitase Lee, Joseph Thomas Repine, Richard William Skeean
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Publication number: 20030064093Abstract: The present invention relates to the discovery of a transdermal delivery system that can deliver high molecular weight pharmaceuticals and cosmetic agents to skin cells. A novel transdermal delivery system with therapeutic and cosmetic application and methods of use of the foregoing is disclosed.Type: ApplicationFiled: June 25, 2002Publication date: April 3, 2003Inventor: Frederick L. Jordan
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Publication number: 20030055051Abstract: The present invention provides an ophthalmic aqueous pharmaceutical preparation, which is excellent in anti-inflammatory effect, which is less stimulative and which has high safety and excellent storage stability. The ophthalmic aqueous pharmaceutical preparation comprises meloxicam and trometamol.Type: ApplicationFiled: May 24, 2002Publication date: March 20, 2003Applicant: WAKAMOTO PHARMACEUTICAL CO., LTD.Inventors: Daisuke Morizono, Hidekazu Suzuki, Masanobu Takeuchi, Kenji Naito
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Patent number: 6509492Abstract: The present invention is directed to methods and compositions for treating upper respiratory indications, such as the treatment, management or mitigation of cough, cold, cold-like symptoms, symptoms related to upper respiratory infections, influenza symptoms and allergic rhinitis, perennial rhinnitis, nasal and Eustachian tube congestion in an animal by administration of tannate compositions comprising combinations of at least one or more agents into a single administrative dose.Type: GrantFiled: September 14, 2001Date of Patent: January 21, 2003Assignee: First Horizon Pharmaceutical CorporationInventor: Balaji Venkataraman
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Publication number: 20020187187Abstract: The present invention relates to a fast disintegrating tablet comprising meloxicam or a pharmaceutically acceptable salt thereof, starch or various starches, glidant and at least one additional excipient.Type: ApplicationFiled: April 17, 2002Publication date: December 12, 2002Inventors: Toshimitsu Ohki, Wakuko Yamaguchi, Kotoe Ohta
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Patent number: 6482846Abstract: Nonsteroidal antiinflammatory drugs which have been substituted with a nitrogen monoxide group; compositions comprising (i) a nonsteroidal antiinflammatory drug, which can optionally be substituted with a nitrogen monoxide group and (ii) a compound that directly donates, transfers or releases a nitrogen monoxide group (preferably as a charged species, particularly nitrosonium); and methods of treatment of inflammation, pain, gastrointestinal lesions and/or fever using the compositions are disclosed. The compounds and compositions protect against the gastrointestinal, renal and other toxicities that are otherwise induced by nonsteroidal antiinflammatory drugs.Type: GrantFiled: August 30, 2001Date of Patent: November 19, 2002Assignee: NitroMed, Inc.Inventors: David S. Garvey, L. Gordon Letts, H. Burt Renfroe, Sang William Tam
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Patent number: 6482814Abstract: A composition comprising a C3-5-alkyl-1,2-benzisothiazolin-3-one and the metal complex of a cyclic thiohydroxamic acid such as the 2:1 zinc salt of either 3-hydroxy-4-methylthiazol-2(3H)-thione or 1-hydroxypyridine-2-thione.Type: GrantFiled: February 15, 2001Date of Patent: November 19, 2002Assignee: Avecia LimitedInventors: Colin Bath, John David Payne, Paula Louise McGeechan
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Patent number: 6440962Abstract: The instant invention is a series of benzothiazine dioxides, or a pharmaceutically acceptable salt thereof, which are potent endothelin A antagonists with profound in vitro activity, and improved syntheses for the Formula I The compounds are useful in treating elevated levels of endothelin, essential renovascular malignant and pulmonary hypertension, cerebral infarction, cerebral ischemia, congestive heart failure, and subarachnoid hemorrhage.Type: GrantFiled: March 27, 2001Date of Patent: August 27, 2002Assignee: Warner-Lambert CompanyInventors: Amy Mae Bunker, Xue-Min Cheng, Annette Marian Doherty, Jeremy John Edmunds, Gerald David Kanter, Chitase Lee, Joseph Thomas Repine, Richard William Skeean
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Patent number: 6440963Abstract: The treatment of neuromuscular dysfunction of the lower urinary tract by compounds which selectively inhibit the COX-2 isozyme is described. The compounds concerned inhibit the COX-2 isozyme with a potency at least 10-fold, and preferably at least 100-fold, greater than their potency on the COX-1 isozyme.Type: GrantFiled: October 1, 2001Date of Patent: August 27, 2002Assignee: Recordati S.A., Chemical and Pharmaceutical CompanyInventors: Amedeo Leonardi, Rodolfo Testa, Luciano Guarneri
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Publication number: 20020115661Abstract: Chronic obstructive pulmonary disease is treated with a selective ETA receptor antagonist such as 4-(7-ethyl-1,3-benxodioxol-5-yl)-2-[2-trifluoromethyl) phenyl]-2H-1,2-benzothiazine-3-carboxylic acid 1,1-dioxide or a pharmaceutically acceptable salt thereof.Type: ApplicationFiled: September 7, 2001Publication date: August 22, 2002Inventors: Laurence Harvey Keller, Milton Lethan Pressler
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Patent number: 6436927Abstract: The present invention involves certain 8-ureido and 8-thioureido, 1,2-benzothiazines, 1,2,4-benzothioxazines and 1,2,4-benzothiodiazines useful in the treatment of disease states mediated by the chemokine, Interleukin-8.Type: GrantFiled: July 7, 1999Date of Patent: August 20, 2002Assignee: SmithKline Beecham CorporationInventors: Hong Nie, Katherine L. Widdowson
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Patent number: 6432945Abstract: This invention is directed to compounds of the formula and the pharmaceutically-acceptable salts thereof, where the substituents are as defined in the Specification, which are growth hormone secretogogues and which increase the level of endogenous growth hormone. The compounds of this invention are useful for the treatment and prevention of osteoporosis and/or frailty, congestive heart failure, frailty associated with aging, obesity; accelerating bone fracture repair, attenuating protein catabolic response after a major operation, reducing cachexia and protein loss due to chronic illness, accelerating wound healing, or accelerating the recovery of burn patients or patients having undergone major surgery; improving muscle strength, mobility, maintenance of skin thickness, metabolic homeostasis or renal homeostasis.Type: GrantFiled: March 30, 2001Date of Patent: August 13, 2002Assignee: Pfizer Inc.Inventors: Philip Albert Carpino, David Andrew Griffith, Bruce Allen Lefker
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Publication number: 20020099049Abstract: Disclosed is a pharmaceutical composition, comprising a combination of a dose of meloxicam or a pharmaceutically acceptable salt thereof and a dose of oxycodone or a pharmaceutically acceptable salt thereof, said combination in an amount sufficient to provide an analgesic effect in a human patient. Also disclosed is a method of effectively treating pain in humans or other mammals, comprising administering to the patient a combination of a dose of meloxicam or a pharmaceutically acceptable salt thereof and a dose of oxycodone or a pharmaceutically acceptable salt thereof such that the dosing interval of the meloxicam overlaps with the dosing interval of the oxycodone, said combination in an amount sufficient to provide an analgesic effect in a human patient.Type: ApplicationFiled: January 25, 2002Publication date: July 25, 2002Inventors: Ronald M. Burch, Richard S. Sackler, Paul D. Goldenheim
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Publication number: 20020094980Abstract: The instant invention is a series of benzothiazine dioxides, or a pharmaceutically acceptable salt thereof, which are potent endothelin A antagonists with profound in vitro activity, and improved syntheses for the Formula 1 1Type: ApplicationFiled: December 5, 2001Publication date: July 18, 2002Inventors: Amy Mae Bunker, Xue-Min Cheng, Annette Marian Doherty, Jeremy John Edmunds, Gerald David Kanter, Chitase Lee, Joseph Thomas Repine, Richard William Skeean