One Of The Cyclos Is A 1,2-thiazine (e.g.,1,2-benzothiazines, Etc.) Patents (Class 514/226.5)
  • Patent number: 6894041
    Abstract: 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 recit
    Type: Grant
    Filed: November 20, 2002
    Date of Patent: May 17, 2005
    Assignee: Pfizer Inc
    Inventors: Anthony Marfat, Michael William McKechney
  • Patent number: 6869945
    Abstract: 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 re
    Type: Grant
    Filed: November 20, 2002
    Date of Patent: March 22, 2005
    Assignee: Pfizer Inc
    Inventors: Anthony Marfat, Michael William McKechney
  • Patent number: 6869948
    Abstract: 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: Grant
    Filed: March 26, 1999
    Date of Patent: March 22, 2005
    Assignee: Boehringer Ingelheim Pharma KG
    Inventors: Thomas Bock, Paul Saegmueller, Peter Sieger, Dietrich Tuerck
  • Patent number: 6867236
    Abstract: 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: Grant
    Filed: April 28, 1999
    Date of Patent: March 15, 2005
    Assignee: Duke University
    Inventors: John C. S. Breitner, Kathleen A. Welsh-Bohmer
  • Patent number: 6844338
    Abstract: 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: Grant
    Filed: May 4, 2001
    Date of Patent: January 18, 2005
    Assignee: Eli Lilly and Company
    Inventors: John Fairhurst, Peter Gallagher
  • Publication number: 20040242571
    Abstract: 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: Application
    Filed: March 15, 2004
    Publication date: December 2, 2004
    Inventors: Alex Haahr Gouliaev, Morgens Larsen, Thomas Varming, Claus Mathiesen, Tina Holm Johansen, Karin Sandager Nielsen, Barbara Hartz, Jorgen Scheel-Kruger
  • Publication number: 20040234596
    Abstract: 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: Application
    Filed: June 28, 2004
    Publication date: November 25, 2004
    Applicant: Boehringer Ingelheim International GmbH
    Inventors: Toshimitsu Ohki, Wakuko Yamaguchi, Kotoe Ohta
  • Patent number: 6811768
    Abstract: 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: Grant
    Filed: October 27, 2003
    Date of Patent: November 2, 2004
    Assignee: The General Hospital Corporation
    Inventors: Warren M. Zapol, Kenneth D. Bloch, Anthony Rosenzweig
  • Publication number: 20040204413
    Abstract: 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: Application
    Filed: January 26, 2001
    Publication date: October 14, 2004
    Inventors: Joaquina Faour, Juan A. Vergez
  • Publication number: 20040180092
    Abstract: Water soluble meloxicam granules comprising:
    Type: Application
    Filed: October 27, 2003
    Publication date: September 16, 2004
    Applicant: Boehringer Ingelheim Vetmedica GmbH
    Inventors: Stefan Henke, Martin Andreas Folger, Jens Schmalz, Diana Christine Keilhofer, Hans-Juergen Kroff, Nina Herz
  • Publication number: 20040176355
    Abstract: 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: Application
    Filed: February 26, 2004
    Publication date: September 9, 2004
    Applicant: Schering Corporation
    Inventors: Thavalakulamgara K. Sasikumar, Wen-Lian Wu, Duane A. Burnett, Li Qiang
  • Publication number: 20040171611
    Abstract: 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: Application
    Filed: September 22, 2003
    Publication date: September 2, 2004
    Applicant: Boehringer Ingelheim Pharma GmbH & Co. KG
    Inventors: Guenter Trummlitz, Rainer Soyka, Peter Sieger, Ulrike Werthmann, Peter Luger
  • Patent number: 6759406
    Abstract: 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 i
    Type: Grant
    Filed: March 25, 2002
    Date of Patent: July 6, 2004
    Assignees: Les Laboratoires Servier, INSERM
    Inventors: Jean-Claude Madelmont, Isabelle Giraud, Colette Nicolas, Jean-Claude Maurizis, Maryse Rapp, Monique Ollier, Pierre Renard, Daniel-Henri Caignard
  • Publication number: 20040127705
    Abstract: A pyrrolesulfonamide derivative having the following formula (I): 1
    Type: Application
    Filed: July 10, 2003
    Publication date: July 1, 2004
    Applicant: DAIICHI PHARMACEUTICAL CO., LTD.
    Inventors: Akira Mizuno, Makoto Shibata, Tomoe Kamei, Harukazu Fukami, Norio Inomata
  • Patent number: 6756370
    Abstract: 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: Grant
    Filed: February 21, 2002
    Date of Patent: June 29, 2004
    Assignee: Merck Patent GmbH
    Inventors: Helmut Prücher, Henning Böttcher, Karl-August Ackermann, Rudolf Gottschlich, Christoph van Amsterdam, Christoph Seyfried, Jürgen Harting, Gerd Bartoszyk, Hartmut Greiner
  • Publication number: 20040116413
    Abstract: The present invention provides compounds of formula I useful as antimicrobial agents 1
    Type: Application
    Filed: November 14, 2001
    Publication date: June 17, 2004
    Inventors: Michael J. Genin, Michael Robert Barbachyn, Jackson B. Hester, Paul D. Johnson, Fred L. Ciske
  • Publication number: 20040110747
    Abstract: 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: Application
    Filed: December 10, 2002
    Publication date: June 10, 2004
    Applicant: Boehringer Ingelheim International GmbH
    Inventor: Raul Altman
  • Publication number: 20040063697
    Abstract: 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: Application
    Filed: June 30, 2003
    Publication date: April 1, 2004
    Inventor: Peter C. Isakson
  • Publication number: 20040063696
    Abstract: 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: Application
    Filed: June 20, 2003
    Publication date: April 1, 2004
    Inventors: Jean-Claude Madelmont, Isabelle Giraud, Aurelien Vidal, Emmanuelle Mounetou, Maryse Rapp, Jean-Claude Maurizis, Pierre Renard, Daniel-Henri Caignard, Jean-Guy Bizot-Espiard
  • Patent number: 6713463
    Abstract: 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: Grant
    Filed: September 27, 2002
    Date of Patent: March 30, 2004
    Assignee: Mucosal Therapeutics, LLC
    Inventors: Stephen T. Sonis, Edward G. Fey
  • Publication number: 20040043992
    Abstract: 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: Application
    Filed: May 21, 2003
    Publication date: March 4, 2004
    Applicant: Boehringer Ingelheim International GmbH
    Inventors: Rene H. Tolba, Yuzo Yamamoto
  • Patent number: 6682747
    Abstract: 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: Grant
    Filed: November 7, 2000
    Date of Patent: January 27, 2004
    Assignee: Boehringer Ingelheim Pharma KG
    Inventors: Dietrich Türck, Veit Schmelmer
  • Publication number: 20030236252
    Abstract: 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: Application
    Filed: November 12, 2002
    Publication date: December 25, 2003
    Inventors: Sham Shridhar Nikam, Ian Leslie Scott, Brian Alan Sherer, Lawrence David Wise
  • Patent number: 6667056
    Abstract: 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: Grant
    Filed: August 20, 2001
    Date of Patent: December 23, 2003
    Assignee: Chiesi Farmaceutici S.p.A.
    Inventors: Paolo Chiesi, Paolo Ventura, Rosa Mezzadri, Gaetano Brambilla, Daniela Acerbi
  • Publication number: 20030232810
    Abstract: 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: Application
    Filed: December 3, 2002
    Publication date: December 18, 2003
    Inventors: Russell Joseph Deorazio, Sham Shridhar Nikam, Ian Leslie Scott, Brian Alan Sherer, Lawrence David Wise
  • Publication number: 20030232787
    Abstract: 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: Application
    Filed: November 26, 2002
    Publication date: December 18, 2003
    Inventor: David James Dooley
  • Patent number: 6664251
    Abstract: 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, sulfonyl
    Type: Grant
    Filed: September 19, 2001
    Date of Patent: December 16, 2003
    Assignee: Daiichi Suntory Pharma Co., Ltd.
    Inventors: Akira Mizuno, Makoto Shibata, Tomoe Iwamori, Norio Inomata
  • Patent number: 6656452
    Abstract: 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: Grant
    Filed: November 14, 1997
    Date of Patent: December 2, 2003
    Assignee: The General Hospital Corporation
    Inventors: Warren M. Zapol, Kenneth D. Bloch
  • Publication number: 20030211163
    Abstract: The invention provides combination therapies for treating papilloma virus.
    Type: Application
    Filed: January 10, 2003
    Publication date: November 13, 2003
    Inventor: Kong Teck Chong
  • Publication number: 20030186973
    Abstract: 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: Application
    Filed: January 21, 2003
    Publication date: October 2, 2003
    Inventor: Joseph Thomas Repine
  • Patent number: 6620853
    Abstract: 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: Grant
    Filed: December 8, 1999
    Date of Patent: September 16, 2003
    Assignees: Mount Sinai School of Medicine, The Rockefeller University
    Inventors: Steven Shiff, Edward A. Fisher, Hayes M. Dansky, Ernane Reis
  • Patent number: 6605627
    Abstract: 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: Grant
    Filed: May 8, 2002
    Date of Patent: August 12, 2003
    Assignee: The Salk Insitute for Biological Studies
    Inventors: Ronald M. Evans, Barry M. Forman
  • Publication number: 20030119825
    Abstract: 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: Application
    Filed: December 9, 2002
    Publication date: June 26, 2003
    Applicant: Boehringer Ingelheim Vetmedica GmbH
    Inventors: Martin Andreas Folger, Stefan Henke, Bernhard Hassel, Bernd Zierenberg
  • Publication number: 20030109520
    Abstract: 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: Application
    Filed: October 22, 2002
    Publication date: June 12, 2003
    Inventors: David S. Garvey, L. Gordon Letts, H. Burt Renfroe, Sang William Tam
  • Patent number: 6562811
    Abstract: 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: Grant
    Filed: September 18, 2001
    Date of Patent: May 13, 2003
    Assignee: Bayer Aktiengesellschaft
    Inventors: 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
  • Publication number: 20030078256
    Abstract: Disclosed are benzothiazine derivatives represented by the following formula (I): 1
    Type: Application
    Filed: September 19, 2001
    Publication date: April 24, 2003
    Applicant: SUNTORY LIMITED
    Inventors: Akira Mizuno, Makoto Shibata, Tomoe Iwamori, Norio Inomata
  • Publication number: 20030073684
    Abstract: 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 1
    Type: Application
    Filed: June 3, 2002
    Publication date: April 17, 2003
    Inventors: Amy Mae Bunker, Xue-Min Cheng, Annette Marian Doherty, Jeremy John Edmunds, Gerald David Kanter, Chitase Lee, Joseph Thomas Repine, Richard William Skeean
  • Publication number: 20030064093
    Abstract: 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: Application
    Filed: June 25, 2002
    Publication date: April 3, 2003
    Inventor: Frederick L. Jordan
  • Publication number: 20030055051
    Abstract: 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: Application
    Filed: May 24, 2002
    Publication date: March 20, 2003
    Applicant: WAKAMOTO PHARMACEUTICAL CO., LTD.
    Inventors: Daisuke Morizono, Hidekazu Suzuki, Masanobu Takeuchi, Kenji Naito
  • Patent number: 6509492
    Abstract: 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: Grant
    Filed: September 14, 2001
    Date of Patent: January 21, 2003
    Assignee: First Horizon Pharmaceutical Corporation
    Inventor: Balaji Venkataraman
  • Publication number: 20020187187
    Abstract: 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: Application
    Filed: April 17, 2002
    Publication date: December 12, 2002
    Inventors: Toshimitsu Ohki, Wakuko Yamaguchi, Kotoe Ohta
  • Patent number: 6482846
    Abstract: 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: Grant
    Filed: August 30, 2001
    Date of Patent: November 19, 2002
    Assignee: NitroMed, Inc.
    Inventors: David S. Garvey, L. Gordon Letts, H. Burt Renfroe, Sang William Tam
  • Patent number: 6482814
    Abstract: 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: Grant
    Filed: February 15, 2001
    Date of Patent: November 19, 2002
    Assignee: Avecia Limited
    Inventors: Colin Bath, John David Payne, Paula Louise McGeechan
  • Patent number: 6440962
    Abstract: 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: Grant
    Filed: March 27, 2001
    Date of Patent: August 27, 2002
    Assignee: Warner-Lambert Company
    Inventors: Amy Mae Bunker, Xue-Min Cheng, Annette Marian Doherty, Jeremy John Edmunds, Gerald David Kanter, Chitase Lee, Joseph Thomas Repine, Richard William Skeean
  • Patent number: 6440963
    Abstract: 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: Grant
    Filed: October 1, 2001
    Date of Patent: August 27, 2002
    Assignee: Recordati S.A., Chemical and Pharmaceutical Company
    Inventors: Amedeo Leonardi, Rodolfo Testa, Luciano Guarneri
  • Publication number: 20020115661
    Abstract: 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: Application
    Filed: September 7, 2001
    Publication date: August 22, 2002
    Inventors: Laurence Harvey Keller, Milton Lethan Pressler
  • Patent number: 6436927
    Abstract: 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: Grant
    Filed: July 7, 1999
    Date of Patent: August 20, 2002
    Assignee: SmithKline Beecham Corporation
    Inventors: Hong Nie, Katherine L. Widdowson
  • Patent number: 6432945
    Abstract: 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: Grant
    Filed: March 30, 2001
    Date of Patent: August 13, 2002
    Assignee: Pfizer Inc.
    Inventors: Philip Albert Carpino, David Andrew Griffith, Bruce Allen Lefker
  • Publication number: 20020099049
    Abstract: 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: Application
    Filed: January 25, 2002
    Publication date: July 25, 2002
    Inventors: Ronald M. Burch, Richard S. Sackler, Paul D. Goldenheim
  • Publication number: 20020094980
    Abstract: 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 1
    Type: Application
    Filed: December 5, 2001
    Publication date: July 18, 2002
    Inventors: Amy Mae Bunker, Xue-Min Cheng, Annette Marian Doherty, Jeremy John Edmunds, Gerald David Kanter, Chitase Lee, Joseph Thomas Repine, Richard William Skeean