Chalcogen Attached Indirectly To The Morpholine Ring By Acyclic Nonionic Bonding Patents (Class 514/238.8)
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Publication number: 20080287443Abstract: Use of a morpholino compound having the general formula (I) wherein R1 is a straight or branched alkyl group containing (8) to (16) carbon atoms at the 2- or 3-position of the morpholino ring, and R2 is a straight or branched alkyl group containing (2) to (10) carbon atoms, substituted with a hydroxy group except in the alpha-position, or a pharmaceutically acceptable salt thereof, in the manufacture of a medicament for the treatment of an infected sub-gingival pocket.Type: ApplicationFiled: November 22, 2006Publication date: November 20, 2008Inventor: Gosta Rutger Persson
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Publication number: 20080280883Abstract: This present invention generally relates to muscarinic receptor antagonists which are useful, among other uses, for the treatment of various diseases of the respiratory, urinary and gastrointestinal systems mediated through muscarinic receptors. The invention also relates to the process for the preparation of disclosed compounds, pharmaceutical compositions containing the disclosed compounds, and the methods for treating diseases mediated through muscarinic receptors.Type: ApplicationFiled: September 23, 2005Publication date: November 13, 2008Inventors: Mohammad Salman, Pakala Kumara Savithru Sarma, Sankaranarayanan Dharmarajan, Anita Chugh, Suman Gupta
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Publication number: 20080269222Abstract: The present invention relates to the use of a morpholino compound having the general formula: (I) wherein R1 is a straight or branched alkyl group containing 8 to 16 carbon atoms at the 2- or 3-position of the morpholino ring, and R2 is a straight or branched alkyl group containing 2 to 10 carbon atoms, substituted with a hydroxy group except in the alpha-position, or pharmaceutically acceptable salts thereof, in the manufacture of a composition for the treatment of acne.Type: ApplicationFiled: July 24, 2006Publication date: October 30, 2008Inventor: Jonathan Douglas Lane
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Publication number: 20080221106Abstract: Disclosed Arylamine ketones of formula (I), their preparation methods, the pharmaceutical compositions containing them and their use in preventing and/or treating the diseases related to the plaque-activating factors, especially in anti-inflammation and immunization, more especially in the treatment of the acute or chronic inflammation, such as, osteoarthritis, oarthritis deformans, etc.Type: ApplicationFiled: August 5, 2005Publication date: September 11, 2008Inventors: Liya Zhu, Wenjie Wang, Halhong Huang, Ziyun Lin, Liyuan Mou, Zhengui Nie, Yu He, Xueyu Ouyang, Shanying Peng, Dongfong Zhang, Jun Wei
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Publication number: 20080206309Abstract: A method of treating menorrhagia and/or dysmenorrhoea in a patient the method comprising administering to the patient an antagonist of a prostaglandin EP2 and/or EP4 receptor. Preferably the patient is a human female.Type: ApplicationFiled: April 14, 2008Publication date: August 28, 2008Applicant: MEDICAL RESEARCH COUNCILInventors: Henry Nicolas JABBOUR, Hilary Octavia Dawn CRITCHLEY
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Publication number: 20080188476Abstract: The present invention relates, in general, to obesity, and, in particular, to a method of treating obesity and minimizing metabolic risk factors associated therewith using, for example, zonisamide or other weight-loss promoting anticonvulsant either alone or in combination with bupropion or other compound that enhances the activity of norepinephrine and/or dopamine via uptake inhibition or other mechanism.Type: ApplicationFiled: May 5, 2006Publication date: August 7, 2008Inventors: Kishore M. Gadde, K. Ranga R. Krishnan
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Publication number: 20080167311Abstract: Novel compounds, and therapeutic methods, compositions and medicament related thereto are disclosed herein.Type: ApplicationFiled: November 13, 2007Publication date: July 10, 2008Inventors: David W. Old, Vinh X. Ngo, Wha-Bin Im
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Publication number: 20080161308Abstract: Compounds of the formula (I): in which A, R1, R2, X, Y and Z are defined in the description, the processes for the preparation of these compounds, the uses thereof for the treatment of dyslipidaemia, atherosclerosis and diabetes, and the pharmaceutical compositions comprising them.Type: ApplicationFiled: December 22, 2005Publication date: July 3, 2008Inventors: Catherine Vidal, Nathalie Adje, Stephane Yvon, Jean Jacques Zeiller
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Publication number: 20080153826Abstract: The present invention is directed to substituted aryl cycloalkanoyl derivatives, compositions containing these derivatives, and methods of their use for the prevention and treatment of conditions ameliorated by monoamine reuptake including, inter alia, vasomotor symptoms (VMS), sexual dysfunction, gastrointestinal and genitourinary disorders, chronic fatigue syndrome, fibromyalgia syndrome, nervous system disorders, and combinations thereof, particularly those conditions selected from the group consisting of major depressive disorder, vasomotor symptoms, stress and urge urinary incontinence, fibromyalgia, pain, diabetic neuropathy, and combinations thereof.Type: ApplicationFiled: February 14, 2008Publication date: June 26, 2008Applicant: WyethInventors: Eugene John Trybulski, Joseph Peter Sabatucci, An Thien Vu, Stephen Todd Cohn, Arthur Attilio Santilli, Lori Krim Gavrin, Fei Ye, Paige Erin Mahaney
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Publication number: 20080096883Abstract: The invention relates to trifluoromethyl substituted benzamide compounds of the formula (I), pharmaceuticals comprising these compounds, their use as or for the manufacture of pharmaceuticals, particularly as inhibitors of protein kinases and/or the treatment of a condition, disorder or disease state mediated by a protein kinase activity and/or a proliferative disease, methods of treatment comprising administering the compounds, especially of therapeutic and prophylactic treatment, methods for the manufacture of the compounds and novel intermediates and partial steps for their synthesis.Type: ApplicationFiled: August 10, 2005Publication date: April 24, 2008Inventors: Giorgio Caravatti, Pascal Furet, Patricia Imbach, Georg Martiny-Baron, Lawrence Blas Perez, Tao Sheng
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Patent number: 7354920Abstract: Compounds of formula (I) wherein Rx is H; Ry is H or C1-C4 alkyl; each Rz is independently H or C1-C4 alkyl; X represents O; Y represents OH or OR; R is C1-C4 alkyl; and Ar1 and Ar2 are optionally substituted phenyl or 5- or 6-membered heteroaryl rings are selective inhibitors of the reuptake of norepinephrine.Type: GrantFiled: August 18, 2003Date of Patent: April 8, 2008Assignee: Eli Lilly and CompanyInventors: Manuel Javier Cases-Thomas, Helen Louise Haughton, Robin George Simmonds, Hélène Catherine Eugénie Rudyk, Magnus Wilhelm Walter, Sivi Ouwerkerk-Mahadevan, John Joseph Masters, Carlos Lamas-Peteira
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Patent number: 7338953Abstract: Disclosed herein are methods of treating an individual suffering from, chronic fatigue syndrome. The methods generally include administration of a therapeutic amount of racemic reboxetine, or a pharmaceutically acceptable salt thereof, to the individual.Type: GrantFiled: February 7, 2006Date of Patent: March 4, 2008Assignee: Pharmacia & Upjohn CompanyInventors: Erik H. F. Wong, Saeeduddin Ahmed, Robert C. Marshall, Robert McArthur, Duncan P. Taylor, Lars Birgerson
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Patent number: 7323466Abstract: The present invention refers to chemical compounds of formula (I) as well as pharmaceutically acceptable salts and esters thereof, wherein R1 to R5 have the significance given in claim 1. These compounds can be used for the preparation of medicaments.Type: GrantFiled: January 13, 2006Date of Patent: January 29, 2008Assignees: Hoffman-La Roche Inc., Vernalis Research LimitedInventors: Jonathan Mark Bentley, Claire Elizabeth Dawson, Wolfgang Guba, Paul Hebeisen, Nathaniel Monck, Robert Mark Pratt, Hans Richter, Stephan Roever, Vicki Ruston
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Patent number: 7317011Abstract: Disclosed herein are methods of treating an individual suffering from peripheral neuropathy. The methods generally include administration of a therapeutic amount of optically pure (S,S) reboxetine, or a pharmaceutically acceptable salt thereof. Embodiments of these methods can diminish adverse side effects.Type: GrantFiled: January 16, 2004Date of Patent: January 8, 2008Assignee: Pharmacia & UpjohnInventors: Erik H. F. Wong, Saeeduddin Ahmed, Robert Clyde Marshall, Robert McArthur, Duncan P. Taylor
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Patent number: 7279478Abstract: This invention relates to class of compounds which are cysteine protease inhibitors, including but not limited to, inhibitors of cathepsins K, L, S and B. These compounds are useful for treating diseases in which inhibition of bone resorption is indicated, such as osteoporosis.Type: GrantFiled: September 3, 2003Date of Patent: October 9, 2007Assignee: Merck Frosst Canada & Co.Inventors: Michael Boyd, Marc Gagnon, Cheuk Lau, Christophe Mellon, John Scheigetz
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Patent number: 7256191Abstract: The subject invention provides compounds which are easily metabolized by the metabolic drug detoxification systems. Particularly, fluvoxamine analogs which have been designed to include esters within the structure of the compounds are taught. Also provided are methods of treating depression and affective disorders, such as obsessive compulsive disorder. Pharmaceutical compositions of the fluvoxamine analogs are also taught.Type: GrantFiled: August 31, 2004Date of Patent: August 14, 2007Assignee: Aryx TherapeuticsInventor: Pascal Druzgala
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Patent number: 7241762Abstract: Disclosed herein are methods of treating an individual suffering from peripheral neuropathy. The methods generally include administration of a therapeutic amount of racemic reboxetine, or a pharmaceutically acceptable salt thereof, to the individual.Type: GrantFiled: February 7, 2006Date of Patent: July 10, 2007Assignee: Pharmacia & Upjohn CompanyInventors: Erik H. F. Wong, Saeeduddin Ahmed, Robert C. Marshall, Robert McArthur, Duncan P. Taylor
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Patent number: 7214701Abstract: The invention relates to insecticidal mixtures for protecting plants against attack by pests comprising (a) compounds of the formula (I) ?in which W, X, Y, Z, A, B, D and G are each as defined in the disclosure, and (b) specified agonists or antagonists of nicotinic acetylcholine receptors.Type: GrantFiled: June 25, 2004Date of Patent: May 8, 2007Assignee: Bayer CropScience AGInventors: Reiner Fischer, Christoph Erdelen
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Patent number: 7166595Abstract: Compounds useful for treating cellular proliferative diseases and disorders by modulating the activity of KSP are disclosed.Type: GrantFiled: May 2, 2003Date of Patent: January 23, 2007Assignees: Cytokinetics, Inc., SmithKline Beecham CorporationInventors: Han-Jie Zhou, David J. Morgans, Jr., Gustave Bergnes, Steven David Knight, Kenneth A. Newlander, Dashyant Dhanak, Nicholas D. Adams
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Patent number: 7166601Abstract: The present invention relates to novel substituted diamine derivatives for the formula wherein R1, R2, R3, R4, X1, X2, X3, X4, A, Y and n are as described in the specification, pharmaceutical compositions containing them and intermediates used in their manufacture. More particularly, the compounds of the invention are motilin receptor antagonists useful for the treatment of associated conditions and disorders such as gastrointestinal reflux disorders, eating disorders leading to obesity and irritable bowel syndrome.Type: GrantFiled: April 26, 2006Date of Patent: January 23, 2007Assignee: Ortho-McNeil Pharmaceutical, Inc.Inventors: Sigmond G. Johnson, Ralph A. Rivero
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Patent number: 7112586Abstract: The present invention relates to novel substituted diamine derivatives for the formula wherein R1, R2, R3, R4, X1, X2, X3, X4, A, Y and n are as described in the specification, pharmaceutical compositions containing them and intermediates used in their manufacture. More particularly, the compounds of the invention are motilin receptor antagonists useful for the treatment of associated conditions and disorders such as gastrointestinal reflux disorders, eating disorders leading to obesity and irritable bowel syndrome.Type: GrantFiled: February 25, 2005Date of Patent: September 26, 2006Assignee: Ortho-McNeil Pharmaceutical, Inc.Inventors: Sigmond G. Johnson, Ralph A. Rivero
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Patent number: 7109198Abstract: The present invention relates, in general, to obesity, and, in particular, to a method of treating obesity and minimizing metabolic risk factors associated therewith using, for example, zonisamide or other weight-loss promoting anticonvulsant either alone or in combination with bupropion or other compound that enhances the activity of norepinephrine and/or dopamine via uptake inhibition or other mechanism.Type: GrantFiled: May 19, 2003Date of Patent: September 19, 2006Assignee: Duke UniversityInventors: Kishore M. Gadde, K. Ranga R. Krishnan
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Patent number: 7098206Abstract: Disclosed is the compound (+)-(2S,3S)-2-(3-chlorophenyl)-3,5,5-trimethyl-2-morpholinol and pharmaceutically acceptable salts and solvates thereof, pharmaceutical compositions comprising them, and processes for their preparation and use; also disclosed is a method of treating depression, attention deficit hyperactivity disorder (ADHD), obesity, migraine, pain, sexual dysfunction, Parkinson's disease, Alzheimer's disease, or addiction to cocaine or nicotine-containing (especially tobacco) products using such compound, salts, solvates or compositions.Type: GrantFiled: May 17, 2002Date of Patent: August 29, 2006Assignee: SmithKline Beecham CorporationInventor: David Lee Musso
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Patent number: 7078402Abstract: The invention relates to novel aminothiol ester compounds having the general formula (I): and to a method for preparing them and to their use in pharmaceutical compositions intended for use in human or veterinary medicine (cancers and precancers, dermatological, rheumatic and ophthalmological complaints in particular) or in cosmetic compositions. The invention also relates to a pharmaceutical or cosmetic composition, characterized in that it comprises, as active agent, a compound of general formula (I) in combination with a pharmaceutically or cosmetically acceptable support.Type: GrantFiled: May 31, 2001Date of Patent: July 18, 2006Assignee: Centre National de la Recherche Scientifique (CNRS)Inventors: Guy Fournet, Gerard Anthony Quash, Jacques Gore
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Patent number: 7078400Abstract: The present invention relates to an inhibitor for production of 20-hydroxyeicosatetraenoic acid, comprising, as an effective ingredient, specific hydroxyformamidine derivatives or pharmaceutically-acceptable salts thereof. The inhibitors according to the present invention are useful as therapeutic agents for kidney diseases, cerebrovascular diseases, or circulatory diseases. In addition, the present invention also provides novel hydroxyformamidine derivatives or pharmaceutically-acceptable salts thereof.Type: GrantFiled: July 1, 2003Date of Patent: July 18, 2006Assignee: Taisho Pharmaceutical Co., Ltd.Inventors: Masakazu Sato, Noriyuki Miyata, Takaaki Ishii, Yuko Kobayashi, Hideaki Amada
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Patent number: 6984652Abstract: Compounds comprising an indazolyl group and a thiazolyl group, preferably 7-substituted 3-(thiazol-2-yl)-1H-indazole compounds in which the indazolyl group and a thiazolyl group are each independently optionally substituted, are useful for the treatment or prophylaxis of bacterial infections in mammals. The compounds are believed to function by inhibiting gyrase B.Type: GrantFiled: May 17, 2004Date of Patent: January 10, 2006Assignee: Warner-Lambert Company LLCInventors: Kraig Yager, Shaosong Chu, Krzysztof Appelt, Xiaoming Li
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Patent number: 6972292Abstract: The present invention relates to certain substituted polyketides of formula I, wherein A, B, C, D, E, F and m are as defined herein, pharmaceutical compositions containing said compounds, and the use of said compounds in treating tumors.Type: GrantFiled: August 5, 2002Date of Patent: December 6, 2005Assignee: Novartis AGInventors: Frederick Ray Kinder, Jr., Kenneth W. Bair, Timothy M. Ramsey, Michael L. Sabio
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Patent number: 6967199Abstract: The present invention relates to novel substituted diamine derivatives for the formula wherein R1, R2, R3, R4, X1, X2, X3, X4, A, Y and n are as described in the specification, pharmaceutical compositions containing them and intermediates used in their manufacture. More particularly, the compounds of the invention are motilin receptor antagonists useful for the treatment of associated conditions and disorders such as gastrointestinal reflux disorders, eating disorders leading to obesity and irritable bowel syndrome.Type: GrantFiled: November 8, 2002Date of Patent: November 22, 2005Assignee: Ortho-McNeil Pharmaceutical, Inc.Inventors: Sigmond G. Johnson, Ralph A. Rivero
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Patent number: 6964782Abstract: Disclosed are several preferred embodiments of hydrogen peroxide which are packaged with ease of use and extended shelf-life in mind. The embodiments include foam, mist, gel, and disposable towelette forms of H2O2. Optional ingredients of topical pain relievers and skin protectants are also disclosed, as are their methods of use.Type: GrantFiled: July 7, 2003Date of Patent: November 15, 2005Assignee: Tec Labs, Inc.Inventors: Robert Lee Smith, Steven Dale Smith, Wendy S. Langley, John Mark Christensen, Vernon W. Smith
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Patent number: 6864254Abstract: An inhibitor for 20-hydroxyeicosatetraenoic acid production which comprises as the active ingredient a specific hydroxyformamidine derivative or a pharmacologically acceptable salt thereof. It is useful especially as a remedy for kidney diseases, cerebrovascular diseases, or circulatory diseases. The novel hydroxyformamidine derivative or pharmacologically acceptable salt thereof is also provided.Type: GrantFiled: November 1, 2000Date of Patent: March 8, 2005Assignee: Taisho Pharmaceutical Co., Ltd.Inventors: Masakazu Sato, Noriyuki Miyata, Takaaki Ishii, Yuko Kobayashi, Hideaki Amada
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Patent number: 6864276Abstract: The invention relates to insecticidal mixtures for protecting plants against attack by pests comprising (a) compounds of the formula (I) ?in which W, X, Y, Z, A, B, D and G are each as defined in the disclosure, and (b) agonists or antagonists of nicotinic acetylcholine receptors.Type: GrantFiled: May 7, 2001Date of Patent: March 8, 2005Assignee: Bayer Cropscience AGInventors: Reiner Fischer, Christoph Erdelen
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Patent number: 6855820Abstract: Disclosed is the compound (+)-(2S,3S)-2-(3-chlorophenyl)-3,5,5-trimethyl-2-morpholinol and pharmaceutically acceptable salts and solvates thereof, methods for preparing them, pharmaceutical compositions comprising them, and processes for their preparation; also disclosed is a method of treating depression, attention deficit hyperactivity disorder (ADHD), obesity, migraine, sexual dysfunction, Parkinson's disease, Alzheimer's disease, or addiction to cocaine or nicotine-containing (especially tobacco) products using such compound, salts, solvates or compositions.Type: GrantFiled: May 17, 2002Date of Patent: February 15, 2005Assignee: SmithKline Beecham CorporationInventors: Toby Broom, Monica Delpogetto, Richard Atkins, Alan Negus, Paul William Oxley
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Patent number: 6812229Abstract: It is to provide a novel fungicide having high controlling effects on plant diseases particularly on wheat powdery mildew and cucumber gray mold, without ill effects on crops. A carbamate derivative represented by the general formula [I] {wherein X is a halogen atom, a C1-C6 alkyl group or the like, n is 0 or an integer of from 1 to 4, R1 is a C1-C6 alkyl group, R2 is a hydrogen atom, a C1-C6 alkyl group or the like, R3 is a hydrogen atom or a C1-C6 alkyl group, G is an oxygen atom, a sulfur atom or the like, Y is a hydrogen atom, a C1-C10 alkyl group, C2-C10 alkenyl group or the like, and Q is a hydrogen atom, a C1-C6 haloalkyl group, a phenyl group or the like} and an agricultural/horticultural fungicide containing the same as the active ingredient.Type: GrantFiled: February 5, 2002Date of Patent: November 2, 2004Assignees: Kumiai Chemical Industry Co., Ltd., Ihara Chemical Industry Co., Ltd.Inventors: Masami Ozaki, Shunichiro Fukumoto, Ryuji Tamai, Kazuhiro Ikegaya, Norihisa Yonekura, Takahiro Kawashima, Junetsu Sakai, Norimichi Muramatsu, Makikazu Takagaki, Kouzou Nagayama
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Publication number: 20040204411Abstract: A method of treating, preventing, or inhibiting a CNS disorder and/or pain and inflammation, or an inflammation-associated disorder in a subject in need of such treatment, prevention, or inhibition provides for treating the subject with reboxetine and a cyclooxygenase-2 selective inhibitor or prodrug thereof, wherein the amount of reboxetine and the amount of a cyclooxygenase-2 selective inhibitor or prodrug thereof together constitute a CNS disorder and/or pain and inflammation or inflammation-associateed disorder suppressing treatment, prevention, or inhibition effective amount of the composition. Compositions and pharmaceutical compositions that contain reboxetine and a cyclooxygenase-2 selective inhibitor are also disclosed.Type: ApplicationFiled: December 4, 2003Publication date: October 14, 2004Applicant: Pharmacia CorporationInventor: Stephen P. Arneric
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Patent number: 6784175Abstract: The use of at least one substituted 1-amino-5-phenylpentane-3-ol and/or 1-amino-6-phenylhexane-3-ol compound and/or one of the enantiomers thereof and/or one of the diastereomers thereof and/or one of the physiologically acceptable salts thereof for producing a medicament that has an N-methyl-D-aspartate-(NMDA)-antagonistic effect.Type: GrantFiled: November 18, 2002Date of Patent: August 31, 2004Assignee: Gruenenthal GmbHInventors: Bernd Sundermann, Werner Englberger, Boris Chizh
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Publication number: 20040147512Abstract: Disclosed are compounds which bind VLA-4. Certain of these compounds also inhibit leukocyte adhesion and, in particular, leukocyte adhesion mediated by VLA-4. Such compounds are useful in the treatment of inflammatory diseases in a mammalian patient, e.g., human, such as asthma, Alzheimer's disease, atherosclerosis, AIDS dementia, diabetes, inflammatory bowel disease, rheumatoid arthritis, tissue transplantation, tumor metastasis and myocardial ischemia. The compounds can also be administered for the treatment of inflammatory brain diseases such as multiple sclerosis.Type: ApplicationFiled: December 29, 2003Publication date: July 29, 2004Applicants: Elan Pharmaceuticals, Inc., American Home Products Corporation.Inventors: Andrei W. Konradi, Michael A. Pleiss, Eugene D. Thorsett, Susan Ashwell, Gregory S. Welmaker, Anthony Kreft, Dimitrios Sarantakis, Darren B. Dressen, Francine S. Grant, Christopher Semko, Ying-Zi Xu
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Patent number: 6756375Abstract: The invention provides for a non-steroidal compound having the formula wherein Re and ′Re are OH, optionally independently etherified or esterified; Z is —CH2— or —CH2CH2—; R1 is H, halogen, CF3, or (1C-4C)alkyl; R2, R3 and R4 are independently H, halogen, —CF3, —OCF3, (1C-8C)Alkyl, hydroxy, (1C-8C)alkyloxy, aryloxy, aryl(1C-8C)alkyl, halo(1C-8C)alkyl, —O(CH2)mX, wherein X is halogen or phenyl and m=2-4; —O(CH2)mNRaRb, —S(CH2)mNRaRb or —(CH2)mNRaRb, wherein m=2-4 and Ra, Rb are independently (1C-8C)alkyl, (2C-8C)alkenyl, (2C-8C)alkynyl, or aryl, optionally substituted with halogen, —CF3, —OCF3, —CN, —NO2, —OH, (1C-8C)alkoxy, aryloxy, carboxyl, (1C-8C)alkylthio, carboxylate, (1C-8C)alkyl, aryl, aryl(1C-8C)alkyl, halo(1C-8C)alkyl or Ra and Rb form a 3-8 membered ring structure, optionally substituted with halogen, —CF3, —OCF3, —CN, —NO2, hydroxy, hydroxy(1C-4C)aType: GrantFiled: July 24, 2003Date of Patent: June 29, 2004Assignee: Akzo Nobel N.V.Inventors: Gerrit Herman Veeneman, Hubert JanJozef Loozen, Jordi Mestres, Eduard Willem De Zwart
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Publication number: 20040110748Abstract: The present invention discloses novel substituted aryl alkylamine compounds of Formula (I) or pharmaceutically acceptable salts thereof which have selective histamine-H3 receptor antagonist activity as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising such cyclic amines as well as methods of using them to treat obesity and other histamine H3 receptor-related diseases.Type: ApplicationFiled: September 18, 2003Publication date: June 10, 2004Inventors: Lisa Selsam Beavers, Robert Alan Gadski, Philip Arthur Hipskind, Craig William Lindsley, Karen Lynn Lobb, James Arthur Nixon, Richard Todd Pickard, John Mehnert Schaus, Takako Takakuwa, Brian Morgan Watson
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Publication number: 20040102440Abstract: Disclosed is a method of promoting smoking cessation in a human comprising administration to the human an effective amount of reboxetine in combination with the administration of a smoking-cessation enhancing agent. Also disclosed is a composition for administration to a human for promoting smoking cessation comprising reboxetine and smoking-cessation enhancing agent. Examples of the smoking-cessation enhancing agents include nicotine, an antidepressant, a nicotine receptor antagonist, and an opioid antagonist.Type: ApplicationFiled: June 24, 2003Publication date: May 27, 2004Inventor: Erik Ho Fong Wong
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Publication number: 20040092516Abstract: Compounds useful for the treatment of various metabolic disorders, such as insulin resistance syndrome, diabetes, hyperlipidemia, fatty liver disease, cachexia, obesity, atherosclerosis and arteriosclerosis, are disclosed.Type: ApplicationFiled: October 14, 2003Publication date: May 13, 2004Inventors: Shalini Sharma, Reid W. von Borstel
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Publication number: 20040092497Abstract: The present invention relates to a class of compounds represented by formula (I) or a pharmaceutically acceptable salt thereof, pharmaceutical compositions comprising compounds of Formula (I), and methods of selectively antagonizing the &agr;&ngr;&bgr;3 and/or the &agr;&ngr;&bgr;5 integrin without significantly antagonizing the IIb/IIIa integrin.Type: ApplicationFiled: September 5, 2003Publication date: May 13, 2004Inventors: Srinivasan Raj Nagarajan, Ish Kumar Khanna, Michael B. Tollefson, Scott B, Mohler, Barbara B. Chen, Mark Russell, Balekudru Devadas, Thomas D. Penning, Lori A. Schretzman, Dale P. Spangler, Mark L. Boys, Nizal S. Chandrakumar, Hwang-Fun Lu
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Publication number: 20040072820Abstract: The instant invention provides novel substituted naphthyl compounds, intermediates, compositions, pharmaceutical formulations, and methods of use.Type: ApplicationFiled: May 27, 2003Publication date: April 15, 2004Inventors: Henry Uhlman Bryant, Thomas Alan Crowell, Charles David Jones, Alan David Palkowitz
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Publication number: 20040062800Abstract: A pharmaceutical composition comprising at least one pharmaceutically active agent that is pH dependent, at least one non-pH dependent sustained release agent, and at least one pH dependent agent that increases the dissolution rate of the at least one pharmaceutically active agent at a pH in excess of 5.5. Such compositions have minimized pH-dependent dissolution profiles or pH-independent dissolution profiles.Type: ApplicationFiled: October 21, 2003Publication date: April 1, 2004Inventors: Beth A. Burnside, Rong-Kun Chang, Xiaodi Guo
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Publication number: 20040058925Abstract: Methods and compositions for treating humans suffering from, or preventing a human from suffering, a physiological or psychiatric disease, disorder, or a condition where inhibiting reuptake of norepinephrine is a benefit are disclosed. The compositions comprise a compound having a pharmacological selectivity of serotonin (Ki)/norepinephrine (Ki) of at least about 5000. Examples of such compounds include reboxetine, and more preferably optically pure (S,S) enantiomer of reboxetine. The methods generally include administration of a therapeutic amount of such compositions. Also disclosed are preparations of a medicament from the composition, and uses of the composition in a manufacture of the medicament to treat a human suffering from, or preventing a human from suffering, a physiological or psychiatric disease, disorder, or condition.Type: ApplicationFiled: September 24, 2003Publication date: March 25, 2004Applicant: PHARMACIA & UPJOHN COMPANYInventors: Erik H.F. Wong, Saeeduddin Ahmed, Robert Clyde Marshall, Robert McArthur, Duncan P. Taylor
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Publication number: 20040058924Abstract: The use of amidoamines to treat or prevent infections attributable to Acanthamoeba and fungi is described. The amidoamines are highly effective against both Acanthamoeba and fungi, and are less toxic to delicate tissues that may become infected with these types of microorganisms (e.g., the cornea).Type: ApplicationFiled: April 30, 2003Publication date: March 25, 2004Inventors: Ronald L. Schlitzer, Nissanke L. Dassanayake, Ruth Ann Rosenthal, Sally L. Buck
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Publication number: 20040048860Abstract: This invention relates to the use of selective noradrenaline reuptake inhibitors, in particular reboxetine, for the treatment of tension-type headache.Type: ApplicationFiled: August 6, 2003Publication date: March 11, 2004Inventors: Jes Olesen, Rigmor Jensen, Lars Bendtsen
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Publication number: 20040029873Abstract: Disclosed are compounds which bind VLA-4. Certain of these compounds also inhibit leukocyte adhesion and, in particular, leukocyte adhesion mediated by VLA-4. Such compounds are useful in the treatment of inflammatory diseases in a mammalian patient, e.g., human, such as asthma, Alzheimer's disease, atherosclerosis, AIDS dementia, diabetes, inflammatory bowel disease, rheumatoid arthritis, tissue transplantation, tumor metastasis and myocardial ischemia. The compounds can also be administered for the treatment of inflammatory brain diseases such as multiple sclerosis.Type: ApplicationFiled: December 11, 2002Publication date: February 12, 2004Inventors: Francine S. Grant, Andrei W. Konradi, Michael A. Pleiss, Eugene D. Thorsett
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Patent number: 6689909Abstract: A compound of formula (I) wherein: n is 1 or 2; R1 is chloro, fluoro, bromo, methyl or methoxy; R2 is as defined within; R3 is as defined within; and R4 is hydrogen or fluoro; or a pharmaceutically acceptable salt or an in vivo hydrolysable ester thereof is described. The use of compounds of formula (I) in the production of an elevation of PDH activity in a warm-blooded animal such as a human being are also described. Pharmaceutical compositions, methods and processes for preparation of compounds of formula (I) are detailed.Type: GrantFiled: June 17, 2002Date of Patent: February 10, 2004Assignee: AstraZeneca ABInventors: Roger John Butlin, Janet Elizabeth Pease, Michael Howard Block, Thorsten Nowak, Jeremy Nicholas Burrows
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Publication number: 20040023961Abstract: This invention relates to methods of using aryl ureas to treat diseases mediated by raf kinase and diseases mediated by the VEGF induced signal transduction pathway characterized by abnormal angiogenesis or hyperpermeability processes.Type: ApplicationFiled: February 11, 2003Publication date: February 5, 2004Applicant: BAYER CORPORATIONInventors: Jacques Dumas, William J. Scott, James Elting, Holia Hatoum-Makdad
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Publication number: 20040019046Abstract: Phenylacetamido-pyrazoles and, more particularly, N-(5-cycloalkyl-1H-pyrazol-3-yl)phenylacetamido derivatives, optionally further substituted as reported in the description; or pharmaceutically acceptable salts thereof; are useful in the treatment of cell proliferative disorders, e.g. cancer, associated with an altered cell cycle dependent kinase activity.Type: ApplicationFiled: May 19, 2003Publication date: January 29, 2004Inventors: Paolo Pevarello, Paolo Orsini, Gabriella Traquandi, Gabriella Brasca, Raffaella Amici, Manuella Villa, Claudia Piutti, Mario Varasi, Antonio Longo