C=x Bonded Directly To The Piperidine Ring (x Is Chalcogen) Patents (Class 514/330)
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Publication number: 20080226618Abstract: This invention relates to compounds of the Formula (I), or a pharmaceutically acceptable salt, solvate, ester or isomer thereof, which is useful for the treatment of diseases or conditions mediated by LpxC.Type: ApplicationFiled: August 29, 2007Publication date: September 18, 2008Inventors: Umar Faruk Mansoor, Panduranga Adulla P. Reddy, M. Arshad Siddiqui
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Patent number: 7425641Abstract: The present invention relates to carboxylic acid amides of general formula wherein R1 to R5, Ar, m and n are defined as in claim 1, the tautomers, stereoisomers, mixtures thereof, the prodrugs and the salts thereof which have valuable properties. The compounds of the above general formula I wherein R5 denotes a cyano group are valuable intermediate products for preparing the other compounds of general formula I, and the compounds of the above general formula I wherein R5 denotes one of the amidino groups mentioned in claim 1 have valuable pharmacological properties, particularly an antithrombotic activity and a factor Xa-inhibiting activity.Type: GrantFiled: September 10, 2004Date of Patent: September 16, 2008Assignee: Boehringer Ingelheim Pharma KGInventors: Uwe Ries, Henning Priepke, Armin Heckel, Herbert Nar, Wolfgang Wienen, Jean Marie Stassen
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Publication number: 20080207640Abstract: The present invention relates to a method of treating cell proliferative disorders by administering to a subject an effective amount of a growth hormone secretagogue compound or a pharmaceutically acceptable salt, hydrate or solvate thereof.Type: ApplicationFiled: February 11, 2008Publication date: August 28, 2008Applicant: Sapphire TherapeuticsInventor: William J. Polvino
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Publication number: 20080200512Abstract: The invention provides a compound of formula: and methods for making and using the same, where R1 and R2 are independently hydrogen, C1-6 alkyl or C1-6 haloalkyl; R3 is hydrogen, halogen, C1-6 alkyl or C1-6 alkoxy; R4 is hydrogen or halogen; and R5 is a mono- or di-amino acid moiety, a succinic acid moiety, a urea moiety, or a derivative thereof. The invention also provides pharmaceutical compositions comprising a compound of formula I, and methods for making and using the same.Type: ApplicationFiled: February 14, 2008Publication date: August 21, 2008Inventors: Jeffrey Mark Blaney, Normand Hebert, Stephanie Ann Hopkins, Elizabeth A. Jefferson, Masaki Tomimoto
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Publication number: 20080200466Abstract: Compounds of formula (I) in free or pharmaceutically acceptable salt form, where R1, R2, R3, R4, R5, R6, R7, m, n, w, X, and Y have the meanings as indicated in the specification, are useful for treating conditions mediated by the CRTh2 receptor, especially inflammatory or obstructive airways diseases.Type: ApplicationFiled: May 22, 2006Publication date: August 21, 2008Inventors: Jake Axford, Urs Baettig, Brian Cox, Kamlesh Jagdis Bala, Catherine Leblanc, David Andrew Sandham
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Publication number: 20080200511Abstract: The present invention relates to novel compounds of Formula (I) wherein ‘X’ represents an amino acid group, ‘n’ is an integer between 1 and 4, ‘R1’ represents benzyl, t-butyl or 9-fluorenylmethyl and ‘R2’ represents a tetramethylmercaptoimidazole derivative or —S+R3R4, wherein R3 and R4 each independently represent lower alkyl, or a pharmaceutically and/or veterinarily acceptable derivative thereof. The present invention further relates to pharmaceutical formulations of said compound and the use thereof in the preparation of a medicament for inhibiting diseases in which transglutaminase has been implicated. Advantageously, the medicament is for treating fibrosis, scarring and/or cancer. Additionally, the invention relates to a method of inhibiting autoimmune diseases such as coeliac disease, neurodegeneration and chronic inflammatory diseases (e.g. of the joints including rheumatoid arthritis and osteoarthritis in a subject).Type: ApplicationFiled: June 16, 2004Publication date: August 21, 2008Applicant: ASTON UNIVERSITYInventors: Martin Griffin, Ian George Coutts, Robert Edward Saint
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Publication number: 20080194537Abstract: The present invention relates to compounds capable of inhibiting binding of the Smac protein to Inhibitors of apoptosis (IAPs). Such compounds are preferably capable of inhibiting IAP and thus may promote apoptosis or sensitize cells for apoptosis. The compounds may be used in the treatment of proliferative diseases, such as cancer.Type: ApplicationFiled: May 23, 2006Publication date: August 14, 2008Inventors: Ole Thastrup, Jens Chr. Norrild
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Publication number: 20080194633Abstract: Chemical entities that modulate smooth muscle myosin and/or non-muscle myosin, pharmaceutical compositions and methods of treatment of diseases and conditions associated with smooth muscle myosin and/or non-muscle myosin are described.Type: ApplicationFiled: August 1, 2007Publication date: August 14, 2008Inventors: Xiangping Qian, Pu-Ping Lu, Chihyuan (Grace) Chuang, Bradley P. Morgan, David J. Morgans
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Publication number: 20080194536Abstract: The present invention relates to a compound represented by the following formula: (I) or a pharmaceutically acceptable salt thereof, or a pharmaceutically acceptable solvate thereof, or a combination thereof, wherein Ro, R1, R1?, R2, R2?, R3 and n are defined herein. The present invention further relates to a method of treating a patient from endometreosis or uterine fibroids.Type: ApplicationFiled: April 14, 2006Publication date: August 14, 2008Inventors: Marlys Hammond, David G. Jones, Istvan Kaldor, Lara S. Kallander, Xi Lang, Scott Kevin Thompson, Philip Stewart Turnbull, David G. Washburn
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Publication number: 20080193492Abstract: This invention relates to novel compositions and methods of use by which the compositions of this invention are applied topically to one or more body parts of at least two individuals who bring said body parts into contact with the other individual and, when said body parts come into contact with each other, permit the formulations to interact and thereby achieve an unexpected sensation to each individual.Type: ApplicationFiled: August 21, 2007Publication date: August 14, 2008Inventors: Nawaz Ahmad, Cheng-Ji Cui, Bryant Ison
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Publication number: 20080167630Abstract: The present invention relates to novel anesthetic compositions containing a non-polymeric carrier material and an anesthetic, where the compositions are suitable for providing a sustained local anesthesia without an initial burst and having a duration for about 24 hours or longer. Certain compositions are also provided that include a first anesthetic and a second anesthetic. In such compositions, the second anesthetic is a solvent for the first anesthetic and provides an initial anesthetic effect upon administration to a subject. The non-polymeric carrier may optionally be a high viscosity liquid carrier material such as a suitable sugar ester. The compositions can further include one or more additional ingredients including active and inactive materials. Methods of using the compositions of the invention to produce a sustained anesthetic effect at a site in a subject are also provided.Type: ApplicationFiled: July 31, 2007Publication date: July 10, 2008Inventor: A. Neil Verity
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Publication number: 20080161325Abstract: The present invention relates to compounds of formula (AA) (I) and (X): useful in treating Alzheimer's disease and other similar diseases. These compounds include inhibitors of the beta-secretase enzyme that are useful in the treatment of Alzheimer's disease and other diseases characterized by deposition of A beta peptide in a mammal. The compounds of the invention are useful in pharmaceutical compositions and methods of treatment to reduce A beta peptide formation.Type: ApplicationFiled: November 13, 2007Publication date: July 3, 2008Inventors: Yvette M. Fobian, John N. Freskos, Barbara Jagodzinska
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Publication number: 20080145434Abstract: Methods of attenuating the toxic or medically undesirable effects of drugs and toxins in a human by administering to a human an injectable formulation comprised of a dispersion of particles comprised of reversed cubic or reversed hexagonal lyotropic liquid crystalline material. The particles absorb or adsorb or otherwise sequester and attenuate the effect of drugs and toxins, and may be used as a rescue or reversal agent, or as a prophylaxis. The invention is especially applicable in reversing adverse effects of local anesthetics inadvertently delivered systemically, and attenuating the therapeutic effects of general anesthetics in the course of treatment.Type: ApplicationFiled: December 6, 2007Publication date: June 19, 2008Inventors: David M. Anderson, Vincent M. Conklin, Benjamin G. Cameransi
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Publication number: 20080146572Abstract: Compounds having the formula are apoptosis promoters. Also disclosed are methods of making the compounds, compositions containing the compounds, and methods of treatment using the compounds.Type: ApplicationFiled: February 26, 2008Publication date: June 19, 2008Applicant: ABBOTT LABORATORIESInventors: Steven W. Elmore, Cheol-Min Park, Xilu Wang
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Publication number: 20080139556Abstract: A composition for binding FKBP proteins is disclosed, along with a method of treating conditions associated with neuronal degeneration, wherein said composition comprises a compound of formula I, wherein, R, R1, R2, R3 and X are as defined herein.Type: ApplicationFiled: December 6, 2006Publication date: June 12, 2008Applicant: AVENTIS PHARMACEUTICALS INC.Inventors: Raymond W. KOSLEY, Bruce Baron, Patrick Jimonet, John G. Jurcak, Stephen J. Shimshock, Xu-yang Zhao, Rosy Sher, Paul J. Mueller, Jennifer Beall, Matthieu Barrague, Joseph W. Guiles
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Publication number: 20080128315Abstract: Biodegradable and resorbable polymer pouches are described for use with cardiac rhythm mamagent devices (CRMs) and other implantable medical devices (IMDs), i.e., a pouch, covering, or other receptacle capable of encasing, surrounding and/or holding the CRM or other IMD for the purpose of securing it in position, inhibiting or reducing bacterial growth, providing pain relief and/or inhibiting scarring or fibrosis on or around the CRM or other IMD. Optionally, the biodegradable and resorbable pouches of the invention include one or more drugs in the polymer matrix to provide prophylactic effects and alleviate side effects or complications associated with the surgery or implantation of the CRM or other IMD.Type: ApplicationFiled: November 6, 2007Publication date: June 5, 2008Applicant: TyRx Pharma, Inc.Inventors: Fatima Buevich, Frank Do, William McJames, William Edelman, Arikha Moses, Mason Diamond
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Publication number: 20080131527Abstract: This invention concerns a synergistic combination of a topical anesthetic and wound barrier forming agent capable of providing extended analgesia of ‘significant open wounds’ (that being, for example, a laceration, surgical incision, abrasion, ulcer or burn, but not being a minor cut, scratch, sting, burn or abrasion) in which conventional management alternatives (such as suturing and/or administration of injected or systemic analgesia) are impractical, unaffordable or otherwise unavailable.Type: ApplicationFiled: September 17, 2007Publication date: June 5, 2008Applicant: ANIMAL ETHICS PTY LTDInventors: Meredith SHEIL, Allan GIFFARD, Charles Robert OLSSON
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Publication number: 20080132480Abstract: The invention relates to substituted phenoxyacetic acids of formula (I), where the variables are as defined in claim 1, as useful pharmaceutical compounds for treating respiratory disorders, pharmaceutical compositions containing them, and processes for their preparation.Type: ApplicationFiled: August 22, 2005Publication date: June 5, 2008Applicant: AstraZeneca ABInventors: Timothy Jon Luker, Timothy Nicholas Birkinshaw, Rukhsana Tasneem Mohammed
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Publication number: 20080132544Abstract: An object of the present invention is to provide a peroxisome proliferator-activated receptor ? (PPAR?) ligand derived from a natural product and to provide a composition for prevention or improvement of insulin resistant syndrome, diabetes mellitus, obesity, or visceral fat obesity, characterized by comprising the ligand as an active ingredient. The present invention provides a PPAR? ligand comprising as an active ingredient, at least one compound selected from the group consisting of coumaperine and derivatives thereof. The present invention also provides a composition for prevention or improvement of insulin resistant syndrome, diabetes mellitus, obesity, or visceral fat obesity comprising the compound as an active ingredient.Type: ApplicationFiled: December 19, 2005Publication date: June 5, 2008Applicant: KANEKA CORPORATIONInventors: Mitsuaki Kitano, Misuzu Tsukagawa, Eisaku Konishi, Tatsumasa Mae, Kazunori Hosoe
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Patent number: 7378440Abstract: The invention relates to substituted benzoylureido-o-benzoylamides and to their physiologically tolerated salts and physiologically functional derivatives. The invention relates to compounds of the formula I in which the radicals have the stated meanings, and to the physiologically tolerated salts thereof. The compounds are suitable for example as medicaments for the prevention and treatment of type 2 diabetes.Type: GrantFiled: July 27, 2004Date of Patent: May 27, 2008Assignee: Sanofi-Aventis Deutschland GmbHInventors: Dieter Kadereit, Elisabeth Defossa, Karl Schoenafinger, Thomas Kalbunde, Andreas Herling
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Patent number: 7375117Abstract: The present invention relates to polypeptides, and nucleic acids DNA encoding these polypeptides, capable of eliciting an immune reaction against cancer, methods for generating T lymphocytes capable of recognizing and destroying tumor cells, and pharmaceutical compositions for the treatment, prophylaxis or diagnosis of cancer.Type: GrantFiled: March 29, 2006Date of Patent: May 20, 2008Assignee: GemVax ASInventors: Gustav Gaudernack, Stein Sæøe-Larssen, Mona Møller, Jon Amund Eriksen
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Patent number: 7368443Abstract: The present invention is directed to 2,6-disubstituted piperidine and piperazine analogs having the following general formula: which are used to treat diseases of the central nervous system, drug abuse, and withdrawal therefrom as well as treating eating disorders.Type: GrantFiled: March 31, 2004Date of Patent: May 6, 2008Assignee: University of Kentucky Research FoundationInventors: Peter A. Crooks, Linda Dwoskin, Marlon D. Jones, Dennis Keith Miller, Seth Davin Norholm, Guangrong Zheng, Sairam Krishamurthy
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Patent number: 7361666Abstract: One aspect of the present invention relates to novel heterocyclic compounds. A second aspect of the present invention relates to the use of the novel heterocyclic compounds as ligands for various cellular receptors, including opiate receptors, other G-protein-coupled receptors, and ion channels. An additional aspect of the present invention relates to the use of the novel heterocyclic compounds as analgesics.Type: GrantFiled: April 11, 2002Date of Patent: April 22, 2008Assignee: Sepracor, Inc.Inventors: Brian M. Aquila, James R. Hauske, Liming Shao
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Patent number: 7358251Abstract: Compounds having the formula are apoptosis promoters. Also disclosed are methods of making the compounds, compositions containing the compounds, and methods of treatment using the compounds.Type: GrantFiled: November 29, 2005Date of Patent: April 15, 2008Assignee: Abbott LaboratoriesInventors: Steven W. Elmore, Cheol-Min Park, Xilu Wang
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Patent number: 7351702Abstract: This invention provides compounds of formula I: wherein Z is oxygen or sulfur; R1 is hydrogen, —CHN2, R, CH2OR, CH2SR, or —CH2Y; next to R3 represents a single or double bond; Y is an electronegative leaving group; R2 is CO2H, CH2CO2H, or esters, amides or isosteres thereof; R3 is a group capable of fitting into the S2 subsite of a caspase enzyme; R4 is a hydrogen or C1-6 alkyl or R3 and R4 taken together form a ring; Ring A and Ring B are each heterocyclic rings, and R and R5 are as described in the specification. The compounds are effective inhibitors of apoptosis and IL-1? secretion.Type: GrantFiled: May 23, 2002Date of Patent: April 1, 2008Assignee: Vertex Pharmaceuticals IncorporatedInventors: Michael Mortimore, Andrew Miller, John Studley, Jean-Damien Charrier
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Patent number: 7351719Abstract: The present invention relates to amide compounds of general formula I wherein the groups and residues A, B, b, W, X, Y, Z, R1, R2 and R3 have the meanings given in claim 1. Moreover the invention relates to pharmaceutical compositions containing at least one amide according to the invention. In view of the MCH receptor-antagonistic activity the pharmaceutical compositions according to the invention are suitable for the treatment of metabolic disorders and/or eating disorders, particularly obesity, bulimia, anorexia, hyperphagia and diabetes.Type: GrantFiled: October 31, 2003Date of Patent: April 1, 2008Assignee: Boehringer Ingelheim Pharma GmbH & Co. KGInventors: Dirk Stenkamp, Stephan Georg Mueller, Gerald Juergen Roth, Philipp Lustenberger, Klaus Rudolf, Thorsten Lehmann-Lintz, Kirsten Arndt, Ralf Lotz, Martin Lenter, Heike-Andrea Wieland
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Patent number: 7351742Abstract: The invention relates to compounds of formula (1) and to processes for the preparation of, intermediates used in the preparation of, compositions containing and the uses of, such derivatives. The compounds according to the present invention are useful in numerous diseases, disorders and conditions, in particular inflammatory, allergic and respiratory diseases, disorders and conditions.Type: GrantFiled: January 19, 2005Date of Patent: April 1, 2008Assignee: Pfizer Inc.Inventors: Alan Daniel Brown, Kim James, Charlotte Alice Louise Lane, Ian Brian Moses, Nicholas Murray Thomson
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Publication number: 20080058336Abstract: The present invention is directed toward substituted hydroxyethylene compounds of formula (XII) useful in treating Alzheimer's disease and other similar diseases.Type: ApplicationFiled: October 10, 2006Publication date: March 6, 2008Inventors: Roy Hom, Shumeye S. Mamo, Jay Tung, Andrea Gailunas, Varghese John, Lawrence Y. Fang
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Publication number: 20080039463Abstract: Compositions of flupirtine for management of neuropathic or inflammatory pain optionally including one or more other analgesics including opiates, NSAIDS and other active agents in immediate and controlled release forms. Methods and systems for administration of these compositions.Type: ApplicationFiled: December 16, 2004Publication date: February 14, 2008Applicant: CNSBio Pty LtdInventors: Raymond Nadeson, Adam Paul Tucker, Colin Goodchild
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Publication number: 20080027035Abstract: The invention relates to compounds of formula (I) wherein Z, R1-5, X, n, A1 and A2 have the meaning as cited in the description and the claims. Said compounds are useful as DPP-IV inhibitors. The invention also relates to the preparation of such compounds as well as the production and use thereof as medicament.Type: ApplicationFiled: December 9, 2004Publication date: January 31, 2008Applicant: GRAFFINITY PHARMACEUTICALS AGInventors: Paul John Edwards, Meritxell Lopez-Canet, Achim Feurer, Silvia Cerezo-Galvez, Victor Ghalio Matassa, Sonia Nordhoff, Meinolf Thiemann, Oliver Hill
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Patent number: 7323563Abstract: A method for the treatment of bacterial infections in humans and non-human mammals, which comprises inhibiting bacterial growth by administering to a subject an antibacterially effective dose of a compound of formula (I) or a pharmaceutically or veterinarily acceptable salt thereof:Type: GrantFiled: August 22, 2005Date of Patent: January 29, 2008Assignee: British Biotech Pharmaceuticals Ltd.Inventors: Michael George Hunter, Paul Raymond Beckett, John Martin Clements, Mark Whittaker, Zoe Marie Spavold
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Patent number: 7309714Abstract: The present invention is directed to phenylalanine derivatives which are inhibitors of the dipeptidyl peptidase-IV enzyme (“DP-IV inhibitors”) and which are useful in the treatment or prevention of diseases in which the dipeptidyl peptidase-IV enzyme is involved, such as diabetes and particularly type 2 diabetes. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which the dipeptidyl peptidase-IV enzyme is involved.Type: GrantFiled: November 26, 2003Date of Patent: December 18, 2007Assignee: Merck & Co., Inc.Inventors: Joseph L. Duffy, Robert J. Mathvink, Ann E. Weber, Jinyou Xu
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Publication number: 20070287730Abstract: This disclosure provides compounds having drug and bio-affecting properties, their pharmaceutical compositions and method of use. In particular, the disclosure is concerned with alkene piperidine derivatives that possess unique antiviral activity. More particularly, the present disclosure relates to compounds useful for the treatment of HIV and AIDS.Type: ApplicationFiled: May 16, 2007Publication date: December 13, 2007Inventors: Tao Wang, Ying Han, John F. Kadow, Zhongxing Zhang, Nicholas A. Meanwell
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Patent number: 7294637Abstract: One aspect of the present invention relates to a method of treating of drug addiction or drug dependence in a mammal, comprising the step of administering to a mammal in need thereof a therapuetically effective amount of a heterocyclic compound, e.g., a 3-substituted piperidine. In a preferred embodiment, the method of the present invention treats cocaine addiction or methamphetamine addiction.Type: GrantFiled: February 4, 2004Date of Patent: November 13, 2007Assignee: Sepracor, Inc.Inventors: Brian M. Aquila, Thomas D. Bannister, Gregory D. Cuny, James R. Hauske, Joanne M. Holland, Paul E. Persons, Heike S. Radeke, Fengjiang Wang, Liming Shao
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Patent number: 7291620Abstract: The present invention is directed to compounds which are inhibitors of the beta-secretase enzyme and which are useful in the treatment or prevention of diseases in which the beta-secretase enzyme is involved, such as Alzheimer's disease. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the treatment of such diseases in which the beta-secretase enzyme is involved.Type: GrantFiled: June 25, 2004Date of Patent: November 6, 2007Assignee: Merck + Co., Inc.Inventors: Craig A. Coburn, Shawn J. Stachel, Joseph P. Vacca, Harold G. Selnick
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Patent number: 7291599Abstract: The invention relates to a process for the treatment of neurodegenerative diseases wherein mis-folded proteins accumulate in characteristic lesions and contribute substantially to a pathogenesis and to an inflammatory reaction magnifying the damage, by the isolated or joint effect of inhibitors of the alanyl amino peptidase (APN) and of the dipeptidyl peptidase N (DP IV). Our results show that the application of inhibitors of the above-referenced enzymes or of preparations and dosage forms containing such inhibitors is definitely suitable for a therapy and prevention of dementia diseases and conditions.Type: GrantFiled: August 11, 2004Date of Patent: November 6, 2007Assignee: Keyneurotek AGInventors: Frank Striggow, Peter Rohnert, Till Mack
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Patent number: 7276511Abstract: The invention provides a compound which exhibits satisfactory peroral absorbability and excellent antagonistic activity against NK-1 receptor or NK-2 receptor.Type: GrantFiled: August 2, 2004Date of Patent: October 2, 2007Assignee: Zeria Pharmaceutical Co., Ltd.Inventors: Masaaki Nagasawa, Nobuo Kawase, Nobuyuki Tanaka, Hideki Nakamura, Naoki Tsuzuike, Masakazu Murata
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Patent number: 7276610Abstract: The invention provides novel GlyT2 inhibiting compounds useful in modulating, treating, or preventing: anxiolytic disorders; a condition requiring treatment of injured mammalian nerve tissue; a condition amenable to treatment through administration of a neurotrophic factor; a neurological disorder; or obesity; an obesity-related disorder.Type: GrantFiled: August 17, 2004Date of Patent: October 2, 2007Assignee: Janssen Pharaceutica, NVInventors: Charles Q. Huang, Timothy W. Lovenberg, Alejandro Santillán, Jr., Liu Y. Tang, Ronald L. Wolin
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Patent number: 7268139Abstract: The invention is directed to methods of bone healing by administering a p38 MAP kinase inhibitor. The invention is directed to methods of treating bone fractures, bone diseases, bone grafting, especially enhancing bone healing following facial reconstruction, maxillary reconstruction, mandibular reconstruction or tooth extraction, enhancing long bone extension, enhancing prosthetic ingrowth, and increasing bone synostosis by administering a p38 MAP kinase inhibitor.Type: GrantFiled: August 29, 2003Date of Patent: September 11, 2007Assignee: Scios, Inc.Inventors: Andrew A. Protter, David Y. Liu, Patrick O'Connor
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Patent number: 7262208Abstract: The present invention relates to compounds of formula (I): useful in treating Alzheimer's disease and other similar diseases. These compounds include inhibitors of the beta-secretase enzyme that are useful in the treatment of Alzheimer's disease and other diseases characterized by deposition of A beta peptide in a mammal. The compounds of the invention are useful in pharmaceutical compositions and methods of treatment to reduce A beta peptide formation.Type: GrantFiled: April 30, 2003Date of Patent: August 28, 2007Assignees: Elan Pharmaceuticals, Inc., Pharmacia & Upjohn CompanyInventors: John A. Tucker, Brian A. Sherer, Ying Zi Xu, Louis Brogley, Shon R. Pulley, Jon S. Jacobs, James P. Beck, Varghese John
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Patent number: 7259157Abstract: Compounds represented by Formula (I): or pharmaceutically acceptable salts thereof, are effective as NMDA NR2B antagonists useful for relieving pain.Type: GrantFiled: April 2, 2002Date of Patent: August 21, 2007Assignee: Merck & Co., Inc.Inventors: Nigel J. Liverton, John W. Butcher, Charles McIntyre, Christopher F. Claiborne, David A. Claremon, John A. McCauley, Joseph J. Romano, Wayne Thompson, Peter M. Munson
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Patent number: 7247748Abstract: Disclosed is a compound having the formula (I) pharmaceutically acceptable salts or solvates thereof and pharmaceutical compositions containing the same, wherein the structural variables are as defined herein.Type: GrantFiled: March 26, 2003Date of Patent: July 24, 2007Assignee: SmithKline CorporationInventors: Scott K. Thompson, James S. Frazee, Lara S. Kallander, Chun Ma, Joseph P. Marino, Michael J. Neeb, Ning Wang
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Patent number: 7244766Abstract: The invention relates to compounds of formula (1) and to processes for the preparation of, intermediates used in the preparation of, compositions containing and the uses of, such derivatives. The compounds according to the present invention are useful in numerous diseases, disorders and conditions, in particular inflammatory, allergic and respiratory diseases, disorders and conditions.Type: GrantFiled: January 19, 2005Date of Patent: July 17, 2007Assignee: Pfizer IncInventors: Alan Daniel Brown, Mark Edward Bunnage, Paul Alan Glossop, Kim James, Charlotte Alice Louise Lane, Russel Andrew Lewthwaite, Ian Brian Moses, David Anthony Price, Nicholas Murray Thomson
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Patent number: 7241810Abstract: The invention relates to compounds of formula (1) and to processes for the preparation of, intermediates used in the preparation of, compositions containing and the uses of, such derivatives. The compounds according to the present invention are useful in numerous diseases, disorders and conditions, in particular inflammatory, allergic and respiratory diseases, disorders and conditions.Type: GrantFiled: March 21, 2005Date of Patent: July 10, 2007Assignee: Pfizer IncInventors: Alan Daniel Brown, Mark Edward Bunnage, Charlotte Alice Louise Lane, Russell Andrew Lewthwaite, Paul Alan Glossop, Kim James, David Anthony Price
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Patent number: 7229969Abstract: Combination of inhibitors of dipeptidyl peptidase IV (DP IV) and enzymes having the same substrate specificity (DP IV-analogous enzymatic activity) and inhibitors of alanyl aminopeptidase (aminopeptidase N, APN) and of enzymes having the same substrate specificity (APN-analogous enzymatic activity) for a more than additive to superadditive inhibition for the treatment of arteriosclerosis, for the treatment of allergic reactions of the type I according to the Gell and Coombs classification and for the treatment of dermatological diseases with follicular and epidermal hyperkeratoses and an enhanced proliferation of keratinocytes.Type: GrantFiled: December 21, 2001Date of Patent: June 12, 2007Assignee: IMTM GmbHInventors: Siegfried Ansorge, Uwe Lendeckel, Klaus Neubert, Dirk Reinhold, Robert Vetter, Harald Gollnick
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Patent number: 7214714Abstract: A hydroxyformamidine compound represented by the following formula or a pharmaceutically acceptable salt thereof [wherein R1 represents a substituted morpholino group, a substituted piperidino group, a piperazin-1-yl group, a substituted piperazin-1-yl group, a thiomorpholin-1-yl group, a perhydroazepin-1-yl group, a perhydroazocin-1-yl group, a tetrahydropyridin-1-yl group, a pyrrolin-1-yl group, etc.; X represents a nitrogen atom or a group represented by CR5; and R2 to R5 are the same or different and each represents a hydrogen atom, a C1-4 alkyl group, a C1-4 alkoxy group, a trifluoromethyl group or a halogen atom.] There is provided a drug which inhibits an enzyme producing 20-HETE participating in a contracting or dilating action for microvessels and an inducing action for cell proliferation in main organs such as kidney and cerebrovascular vessels.Type: GrantFiled: April 26, 2002Date of Patent: May 8, 2007Assignee: Taisho Pharmaceutical Co. Ltd.Inventors: Masakazu Sato, Noriyuki Miyata, Takaaki Ishii, Yuko Matsunaga, Hideaki Amada
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Patent number: 7202282Abstract: The subject invention provides microemulsions having, as one component thereof, electron-deficient aromatic rings, e.g.. di(trifluoromethyi) benzene, for efficient separation and/or isolation of target molecules, e.g., bupivacaine.Type: GrantFiled: April 22, 2003Date of Patent: April 10, 2007Assignee: University of FloridaInventors: Donn M. Dennis, Timothy E. Morey, Richard E. Partch, Dinesh O. Shah, Manoj Varshney
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Patent number: 7199243Abstract: PPAR alpha activators, pharmaceutical compositions containing such compounds and the use of such compounds to elevate certain plasma lipid levels, including high density lipoprotein-cholesterol and to lower certain other plasma lipid levels, such as LDL-cholesterol and triglycerides and accordingly to treat diseases which are exacerbated by low levels of HDL cholesterol and/or high levels of LDL-cholesterol and triglycerides, such as atherosclerosis and cardiovascular diseases, in mammals, including humans.Type: GrantFiled: November 24, 2003Date of Patent: April 3, 2007Assignees: Pfizer Inc., Pfizer Products Inc.Inventors: Scott W. Bagley, Thomas A. Brandt, Robert W. Dugger, William A. Hada, Cheryl M. Hayward, Zhengyu Liu
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Patent number: 7196103Abstract: The present invention is directed to the compound of formula I which is useful for inhibiting the activity of Factor Xa. The present invention is also directed to compositions containing said compounds, processes for their preparation, their use, such as for inhibiting the formation of thrombin or for therapeutically or prophylactically treating a patient suffering from, or subject to, or associated with a disease state associated with a cardiovascular disorder.Type: GrantFiled: May 19, 2004Date of Patent: March 27, 2007Assignee: Sanofi-Aventis Deutschland GmbHInventors: Marc Nazare, Volkmar Wehner, Kurt Ritter, Volker Laux
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Patent number: 7173045Abstract: The invention concerns 4-aminomethyl-1-aryl-cyclohexylamine compounds, methods for producing same, pharmaceutical formulations containing said compounds and the use of 4-aminomethyyl-1-aryl-cyclohexylamine compounds for producing medicines and in related methods of treatment.Type: GrantFiled: May 10, 2005Date of Patent: February 6, 2007Assignee: Gruenenthal GmbHInventors: Bernd Sundermann, Hans Schick, Claudia Hinze