Q Contains Benzene Ring Patents (Class 514/602)
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Patent number: 7375120Abstract: Novel PDF inhibitors and novel methods for their use are provided.Type: GrantFiled: April 16, 2003Date of Patent: May 20, 2008Assignee: Smithkline Beecham CorporationInventors: Siegfried B. Christensen, IV, Maxwell D. Cummings, Jinhwa Lee, Jia-ning Xiang
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Publication number: 20080113030Abstract: A sustained release tamsulosin formulation contains tamsulosin, a hydrophobic polymer, a microsphere forming agent and a diluent. The hydrophobic polymers include pH-dependent and pH-independent polymers are used as the release-modulating agent to control the dissolution profile of tamsulosin formulation so that the formulation releases tamsulosin slowly and continuously as the formulation passed through the stomach and gastrointestinal tract. The present invention further relates to a method for preparing the sustained release tamsulosin formulation.Type: ApplicationFiled: November 9, 2006Publication date: May 15, 2008Inventors: Ching-Fen Hsiao, Sung-Jen Chen, Ya-Ching Chang Chien
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Patent number: 7361787Abstract: The present invention relates to novel compounds of formula (I), to a process for their manufacture, to pharmaceutical compositions containing them, and to their use in therapy, in particular their use in the prophylaxis and treatment of respiratory diseasesType: GrantFiled: September 11, 2002Date of Patent: April 22, 2008Assignee: Glaxo Group LimitedInventors: Philip Charles Box, Diane Mary Coe, Brian Edgar Looker, Panayiotis Alexandrou Procopiou
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Patent number: 7339078Abstract: Selected bis-amino acid hydroxyethylamino sulfonamide compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease. The present invention relates to such retroviral protease inhibitors and, more particularly, relates to selected novel compounds, compositions, and methods for inhibiting retroviral proteases, such as human immunodeficiency virus (HIV) protease, prophylactically preventing retroviral infection or the spread of a retrovirus, and treatment of a retroviral infection.Type: GrantFiled: August 10, 2006Date of Patent: March 4, 2008Assignee: G.D. Searle LLCInventors: Daniel P Getman, Gary A DeCrescenzo, John N Freskos, Michael L Vazquez, James A Sikorski, Balekudru Devadas, Srinivasan Raj Nagarajan, David L Brown, Joseph J McDonald
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Publication number: 20080051330Abstract: Novel compositions and methods of treating and preventing a viral infection are provided. A method of blocking a viral infection facilitated by a serine proteolytic (SP) activity is disclosed, which involves administering to a subject suffering or about to suffer from a viral infection a therapeutically effective amount of a substance having serine protease inhibitory activity or serpin activity. Among the substances found to be useful are ?1-antitrypsin (AAT), peptide derivatives from the carboxy terminal end of AAT and synthetic drugs mimicking the action of such substances. The invention is particularly well suited for checking a viral infection mediated by members of herpesviridae family.Type: ApplicationFiled: April 14, 2006Publication date: February 28, 2008Inventor: Leland Shapiro
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Patent number: 7332175Abstract: A pharmaceutical composition comprising: (a) an anticholinergic of formula 1 ?wherein X? is an anion with a single negative charge; and (b) a compound of formula 2 ?or the pharmacologically acceptable acid addition salts, solvates, and hydrates thereof.Type: GrantFiled: April 16, 2004Date of Patent: February 19, 2008Assignee: Boehringer Ingelheim International GmbHInventor: Ingo Konetzki
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Publication number: 20080027073Abstract: The present invention refers to new indanyl sulphonamide compounds with general formula (I), as well as to their preparation procedure, their application as medicine and the pharmaceuticals composition which they are made up of. The new compounds of formula I show affinity for 5-HT6 receptors and are, therefore, effective for treating diseases mediated by these receptors.Type: ApplicationFiled: August 18, 2006Publication date: January 31, 2008Applicant: Laboratorios Del Dr. Esteve, S.A.Inventors: Maria De Las Ermitas Alcalde-Pais, Maria De Les Neus Mesquida-Estevez, Sara Lopez-Perez, Jordi Frigola-Constansa, Joerg Holenz, Ramon Merce-Vidal
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Patent number: 7321001Abstract: Compounds, pharmaceutical compositions and methods are provided that are useful in the treatment of inflammatory and immune-related diseases and conditions. In particular, the invention provides compounds which modulate the function and/or expression of proteins involved in atopic diseases, inflammatory conditions and cancer. The subject compounds are carboxylic acid derivatives.Type: GrantFiled: December 19, 2003Date of Patent: January 22, 2008Assignee: Amgen Inc.Inventors: Zice Fu, Xi Alan Huang, Jiwen Liu, Julio C. Medina, Michael J. Schmitt, H. Lucy Tang, Yingcai Wang, Qingge Xu
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Patent number: 7312248Abstract: Novel trifluoromethanesulfonanilide oxime ether compounds useful for controlling endo and/or ectoparasites in the environment are provided, together with methods of making the same, and methods of using the inventive compounds to treat parasite infestations in vivo or ex vivo.Type: GrantFiled: September 21, 2005Date of Patent: December 25, 2007Assignee: Schering-Plough Animal Health CorporationInventors: Adam Gerhard Meyer, Kevin Norman Winzenberg, David G. Sawutz, Andris Juris Liepa
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Publication number: 20070287750Abstract: Certain lipophilic polycationic sulfonamides are provided and are useful for treating various diseases or conditions and particularly sepsis.Type: ApplicationFiled: June 7, 2006Publication date: December 13, 2007Applicants: The University of Kansas, MediQuest Therapeutics, Inc.Inventors: Mark R. Burns, Sunil A. David, Scott A. Jenkins
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Publication number: 20070281978Abstract: This invention relates an inhibitory modulator of AQP4 protein regarding its transmembrane water transport properties, wherein the modulator selectively binds to the AQP4 protein, and inhibits AQP4 mediated water transport.Type: ApplicationFiled: June 1, 2007Publication date: December 6, 2007Applicant: NIIGATA UNIVERSITYInventors: Tsutomu Nakada, Vincent J. Huber
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Patent number: 7297796Abstract: Novel sulfamoyl benzamide compounds, pharmaceutical compositions containing the sulfamoyl benzamide compounds, and methods of their pharmaceutical use are disclosed. In certain embodiments, the sulfamoyl benzamide compounds are agonists and/or modulating ligands of cannabinoid receptors and may be useful, inter alia, for treating and/or preventing pain, gastrointestinal disorders, inflammation, auto-immune diseases, ischemic conditions, immune-related disorders, hypertension, neurological disorders, and neurodegenerative diseases, for providing cardioprotection against ischemic and reperfusion effects, for inducing apoptosis in malignant cells, for inhibiting mechanical hyperalgesia associated with nerve injury, and as an appetite stimulant.Type: GrantFiled: October 13, 2005Date of Patent: November 20, 2007Assignee: Adolor CorporationInventors: Roland E. Dolle, Karin Worm, Q. Jean Zhou
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Patent number: 7291634Abstract: The invention relates to ?-amino-N-hydroxy-acetamide derivatives of formula I, wherein R is di-lower alkyl amino, 1,2,3-triazol-1-yl, 1,2,3-triazol-2-yl or 1,2,4-triazol-4-yl, m represents an integer from 1 up to and including 10, and n represents an integer from 0 up to and including 10, and salts thereof; to processes for their preparation, pharmaceutical compositions comprising said hydroxamic acid derivatives, the use of such hydroxamic acid derivatives as medicaments, and a method of treating conditions or diseases mediated by matrix-degrading metalloproteinases (MMP's) using said derivatives alone or in combination with one or more other therapeutic agents.Type: GrantFiled: August 7, 2006Date of Patent: November 6, 2007Assignee: Novartis AGInventors: Kenji Hayakawa, Genji Iwasaki, Shinichi Koizumi, Ichiro Umemura
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Publication number: 20070249723Abstract: Methods for preparing substituted phenylsulfonamide compounds of the following structure are provided: or a pharmaceutically acceptable salt thereof, wherein, R1-R7 are defined herein. Also provided are methods for preparing compounds of the following structure: wherein, R9, m, n, p, r, and s are defined herein.Type: ApplicationFiled: April 19, 2007Publication date: October 25, 2007Applicant: WyethInventors: Asaf Ragim Alimardanov, Jean Schmid, Jay Thomas Afragola, Gulnaz Khafizova
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Publication number: 20070249722Abstract: A compound of Formula (I), or pharmaceutically acceptable salts and/or hydrates or prodrugs thereof, wherein Formula (I) has the structure: is provided, wherein R1-R7 are defined herein. These compounds are useful in medicaments for treating a disease selected from the group consisting of Alzheimer's Disease, amyloid angiopathy, cerebral amyloid angiopathy, systemic amyloidosis, hereditary cerebral hemorrhage with amyloidosis of the Dutch type, inclusion body myositis, mild cognitive impairment (MCI) and Down's syndrome, in a subject.Type: ApplicationFiled: April 19, 2007Publication date: October 25, 2007Applicant: WyethInventors: Alexander Michael Porte, Thomas Joseph Caggiano, George Diamantidis, Diane Barbara Hauze, Boyd Lynn Harrison, Molly Hoke, Anthony Kreft, Dennis M. Kubrak, Charles William Mann, Scott Mayer, Koi Michele Morris
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Patent number: 7285565Abstract: Novel benzamide compounds, their salts and compositions related thereto having activity against mammalian factor Xa are disclosed. The compounds are useful in vitro or in vivo for preventing or treating coagulation disorders.Type: GrantFiled: January 14, 2005Date of Patent: October 23, 2007Assignee: Millennium Pharmaceuticals, Inc.Inventors: Bing-Yan Zhu, Penglie Zhang, Lingyan Wang, Wenrong Huang, Erick A. Goldman, Wenhao Li, Jingmei Zuckett, Yonghong Song, Robert M. Scarborough
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Patent number: 7271195Abstract: Disclosed herein are carbonyl compounds of Formula I, II, or III, and others as described herein. Also disclosed are methods of treating disease, such as cancer, neurological disorders, including polyglutamine-repeat disorders, anemias, thalassemias, inflammatory conditions, autoimmune diseases and cardiovascular conditions, using the compounds of the invention. In addition, methods of modulating the activity of histone deacetylase (HDAC) are also disclosed.Type: GrantFiled: June 10, 2004Date of Patent: September 18, 2007Assignee: Kalypsys, Inc.Inventors: Paul L. Wash, Brandon M. Wiley, Christian Hassig, James W. Malecha, Stewart A. Noble
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Patent number: 7265130Abstract: The present invention provides a pharmaceutical composition for use as an NPY Y5 receptor antagonist comprising a compound of the formula (I): wherein R1 is lower alkyl, cycloalkyl or the like, R2 is hydrogen, lower alkyl or the like, n is 1 or 2, X is lower alkylene, lower alkenylene, arylene, cycloalkylene or the like, Y is CONR7, CSNR7, NR7CO, NR7CS or the like, Z is lower alkyl, optionally substituted carbocyclyl, optionally substituted heterocyclyl or the like and R7 is hydrogen or lower alkyl, prodrug, pharmaceutically acceptable salt or solvate thereof.Type: GrantFiled: December 30, 2003Date of Patent: September 4, 2007Assignee: Shionogi & Co., Ltd.Inventors: Yasuyuki Kawanishi, Hideyuki Takenaka, Kohji Hanasaki, Tetsuo Okada
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Patent number: 7265220Abstract: Compound of formula (I): wherein: R1 represents aryl, heteroaryl or alkyl which is optionally substituted, or a group of formula —(CO)—CR6R7NR8R9 wherein R6, R7, R8 and R9 are as defined in the description, R2 represents hydrogen or alkyl, R3 represents hydrogen or optionally substituted alkyl, R4 represents a saturated or unsaturated, 7- to 15-membered bicyclic system or optionally substituted alkyl, or R3 and R4, together with the carbon atom carrying them, form a saturated or unsaturated, 3- to 18-membered, mono-, bi- or tri-cyclic system optionally containing one or more hetero atoms selected from O, S and N and optionally substituted, n represents 1 or 2, Ar represents aryl or heteroaryl, R5 represents amino, guanidino, cyano or amidino which is optionally substituted, its optical isomers, and also addition salts thereof with a pharmaceutically acceptable acid. Medicinal products containing the same which are useful in pathological conditions involving activated protein C.Type: GrantFiled: February 17, 2003Date of Patent: September 4, 2007Assignee: Les Laboratories ServierInventors: Guillaume De Nanteuil, Philippe Gloanec, Tony Verbeuren, Alain Rupin
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Patent number: 7256204Abstract: A compound of the formula: wherein Ar is an aromatic ring assembly group which may be substituted or a fused aromatic group which may be substituted; X is (i) a bond, (ii) —S—, —SO— or —SO2—, (iii) C1-6 alkylene, C2-6 alkenylene or C2-6 alkynylene, etc.Type: GrantFiled: August 21, 2003Date of Patent: August 14, 2007Assignee: Takeda Pharmaceutical Company LimitedInventors: Kaneyoshi Kato, Jun Terauchi, Hiroaki Fukumoto, Mitsuru Kakihana
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Patent number: 7227035Abstract: Compounds are provided that act as potent antagonists of chemokine receptors. The compounds are generally aryl sulfonamide derivatives and are useful in pharmaceutical compositions, methods for the treatment of chemokine receptor-mediated diseases, and as controls in assays for the identification of chemokine antagonists.Type: GrantFiled: May 19, 2004Date of Patent: June 5, 2007Assignee: ChemocentryxInventors: Solomon Ungashe, Zheng Wei, J. J. Wright, Andrew Pennell, Brett Permack, Thomas Schall
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Patent number: 7208526Abstract: The present invention relates to the compounds of formula I: their pharmaceutically acceptable salts or esters, enantiomeric forms, diastereoisomers and racemates, the preparation of the above compounds, pharmaceutical compositions containing them and their manufacture, as well as the use of such compounds in the control or prevention of illnesses such as cancer.Type: GrantFiled: April 28, 2006Date of Patent: April 24, 2007Assignee: Hoffmann-La Roche Inc.Inventors: Edward Boyd, Frederick Brookfield, Jonathan Gridley, Matthias Koerner, Manfred Kubbies, Raymond Lau, Ulrike Reiff, Georg Tiefenthaler, Wolfgang von der Saal, Timothy Woodcock
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Patent number: 7208528Abstract: Novel inhibitors of polyamine transport having inhibition constants two orders of magnitude lower than those of known compounds are disclosed. These polyamine analogues are useful pharmaceutical agents for treating diseases where it is desired to inhibit polyamine transport or other polyamine binding proteins, for example cancer and post-angioplasty injury. Novel chemical synthetic methods to obtain polyamine analogues are disclosed, including the production of a combinational polyamine library. These approaches yield analogues with desirable activities both for diagnostic and research assays and therapy. The assays of the invention are useful for high throughput screening of targets in the discovery of drugs that interact with the polyamine system.Type: GrantFiled: September 15, 1999Date of Patent: April 24, 2007Assignee: MediQuest Therapeutics, Inc.Inventors: Nicolaas M. J. Vermeulin, Christine L. O'Day, Heather K. Webb, Mark R. Burns, Donald E. Bergstrom
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Patent number: 7205434Abstract: There is disclosed a novel class of sulphonamido-substituted bridged bicycloalkyl derivatives comprising a substitute on the bridgehead position. The compounds modulate the production of the ?-amyloid precursor protein, and hence are useful in the treatment of Alzheimer's Disease.Type: GrantFiled: July 31, 2002Date of Patent: April 17, 2007Assignee: Merck Sharp & Dohme Ltd.Inventors: Joanne Clare Hannam, Timothy Harrison, Andrew Madin, Timothy Jason Sparey
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Patent number: 7192940Abstract: The present invention relates to novel ether compounds, compositions comprising ether compounds, and methods useful for treating and preventing cardiovascular diseases, dyslipidemias, dysproteinemias, and glucose metabolism disorders comprising administering a composition comprising an ether compound. The compounds, compositions, and methods of the invention are also useful for treating and preventing Alzheimer's Disease, Syndrome X, peroxisome proliferator activated receptor-related disorders, septicemia, thrombotic disorders, obesity, pancreatitis, hypertension, renal disease, cancer, inflammation, and impotence. In certain embodiments, the compounds, compositions, and methods of the invention are useful in combination therapy with other therapeutics, such as hypocholesterolemic and hypoglycemic agents.Type: GrantFiled: July 16, 2004Date of Patent: March 20, 2007Assignee: Esperion Therapeutics, Inc.Inventors: Jean-Louis Henri Dasseux, Carmen Daniela Oniciu
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Patent number: 7166622Abstract: Compounds of Formula I, wherein R1–R8 are defined herein are provided, together with pharmaceutically acceptable salts, hydrates, metabolites, and/or prodrugs thereof. Uses of these compounds for inhibiting beta amyloid production and for the prevention and treatment of Alzheimer's Disease and Down's syndrome are described.Type: GrantFiled: June 9, 2003Date of Patent: January 23, 2007Assignees: Wyeth, ArQule, Inc.Inventors: Anthony Frank Kreft, Derek Cecil Cole, Kevin Roger Woller, Joseph Raymond Stock, Kristina Martha Kutterer, Dennis Martin Kubrak, Charles William Mann, William Jay Moore, David Scott Casebier
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Patent number: 7161031Abstract: Compounds useful as antiproliferative agents, including, for example, anticancer agents, are provided according to formula I: wherein: Ar, X, X1, g, R and R3 are as defined herein.Type: GrantFiled: February 28, 2003Date of Patent: January 9, 2007Assignees: Temple University - Of The Commonwealth System of Higher Education, Onconova Therapeutics, Inc.Inventors: E. Premkumar Reddy, M.V. Ramana Reddy, Stanley C. Bell
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Patent number: 7160923Abstract: Novel inhibitors of polyamine transport having inhibition constants two orders of magnitude lower than those of known compounds are disclosed. These polyamine analogues are useful pharmaceutical agents for treating diseases where it is desired to inhibit polyamine transport or other polyamine binding proteins, for example cancer and post-angioplasty injury. Novel chemical synthetic methods to obtain polyamine analogues are disclosed, including the production of a combinatiorial polyamine library. These approaches yield analogues with desirable activities both for diagnostic and research assays and therapy. The assays of the invention are useful for high throughput screening of targets in the discovery of drugs that interact with the polyamine system.Type: GrantFiled: November 14, 2000Date of Patent: January 9, 2007Assignee: MediQuest Therapeutics, Inc.Inventors: Nicolaas M. J. Vermeulin, Christine L. O'Day, Heather K. Webb, Mark R. Burns, Donald E. Bergstrom
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Patent number: 7157454Abstract: The invention relates to compounds of formula: These compounds show affinity for the bradykinin receptors with selectivity towards the B1 receptors; they may be used for the preparation of medicinal products intended for treating or preventing inflammation pathologies and persistent or chronic inflammatory diseases.Type: GrantFiled: March 27, 2002Date of Patent: January 2, 2007Assignee: Sanofi-AventisInventors: Bernard Ferrari, Jean Gougat, Yvette Muneaux, Pierre Perreaut, Lionel Sarran
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Patent number: 7157498Abstract: The invention concerns diamines of general formula (I), wherein: A represents a group A1 or A2 of general formula (II); B represents a group B1 or B2 of general formula (III); X represents a SO2, CH2, C?O or COO; YZ represents a group of formula CH(R25)—CH(R26) or CH(R27)?(R28), and R1 to R28, identical or different, represent independently of one another, a hydrogen or halogen atom or an alkyl, cycloalkyl, CN, NO2, hydroxy, aryl, aralkyl, alkoxy, aryloxy, amino, alkylamino, dialkylamino, cycloalkylamino, arylamino, arylalkylamino, diarylamino diarylalkylamino, trihalogenoalkyl or trihalogenoalkoxy group, provided that in the group A1, at least one of the radicals R1, R2, R3, R4 or R5 represents the hydrogen atom when the other four do not represent the hydrogen atom and in the group B1, at least one of the radicals R13, R14, R15, R16 or R17 represents the hydrogen atom when the other four do not represent the hydrogen atom, and their salts with a pharmaceutically acceptable acid, in the form of racemic mixtuType: GrantFiled: August 7, 2001Date of Patent: January 2, 2007Assignee: Centre National de la Recherche Scientifique (CNRS)Inventors: Philippe Marcel Dauban, Robert Hugh Dodd, Helene Veronique Faure, Martial Ruat, Pierre Jean-Paul Potier, Albane Kessler
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Patent number: 7148233Abstract: Methods for treating cardiovascular and related diseases such as hypertrophy are described. The methods are directed to concurrently administering a compound such as pyridoxal-5?-phosphate, pyridoxamine, pyridoxal, or a 3-acylated pyridoxal analogue with a therapeutic cardiovascular compound.Type: GrantFiled: August 12, 2003Date of Patent: December 12, 2006Assignee: Merrill Lynch Capital Canada Inc.Inventors: Rajat Sethi, Wasimul Haque
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Patent number: 7144892Abstract: Methods for treating cardiovascular and related diseases such as myocardial infarction are described. The methods are directed to concurrently administering a compound such as pyridoxal-5?-phosphate, pyridoxamine, pyridoxal, or a 3-acylated pyridoxal analogue with a therapeutic cardiovascular compound.Type: GrantFiled: August 12, 2003Date of Patent: December 5, 2006Assignee: Merrill Lynch Capital Canada Inc.Inventors: Rajat Sethi, Wasimul Haque
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Patent number: 7138432Abstract: ?-Amino hydroxamic acid derivative of formula (I), in which R is C2–C7-alkyl, which is mono-, di- or trisubstituted by halogen, nitro, lower acyloxy, trifluoromethoxy, cyano, C3–C5-cycloalkyl or unsubstituted or substituted C3–C4-heteroaryl comprising one or two heteroatoms selected from the group consisting of O, S and N; or C3–C7-alkenyl or C3–C7-alkynyl, which in each case is unsubstituted or mono-, di- or trisubstituted by halogen, nitro, lower acyloxy, trifluoromethoxy, cyano, C3–C5-cycloalkyl or unsubstituted or substituted C3–C6-heteroaryl comprising one or two heteroatoms selected from the group consisting of O, S and N; and the other symbols are as defined in claim 1, are described. These compounds are MMP and in particular MMP2 inhibitors and can be used for treatment of MMP dependent diseases, in particular inflammation conditions, rheumatoid arthritis, osteoarthritis, tumors (tumor growth, metastasis, progression or invasi n) and pulmonary disorders (e.g. emphysema, COPD).Type: GrantFiled: August 7, 2000Date of Patent: November 21, 2006Assignee: Novartis AGInventors: Werner Breitenstein, Kenji Hayakawa, Genji Iwasaki, Takanori Kanazawa, Tatsuhiko Kasaoka, Shinichi Koizumi, Shinichiro Matsunaga, Motowo Nakajima, Junichi Sakaki
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Patent number: 7135487Abstract: The present invention relates to novel sulphonamide derivatives, to processes for their preparation and to pharmaceutical compositions containing them.Type: GrantFiled: May 29, 2003Date of Patent: November 14, 2006Assignee: Eli Lilly and CompanyInventors: Macklin B Arnold, Stephen R Baker, Thomas J Bleisch, Buddy E Cantrell, Ana M Escribano, Ken Matsumoto, Tracey E McKennon, Paul L Ornstein, Richard L Simon, Edward C. R. Smith, Hamideh Zarrinmayeh, Dennis M Zimmerman
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Patent number: 7122571Abstract: Compounds useful as inhibitors of cyclooxygenase-2 activity have the formulae I or Ia: wherein: Q1, Q2, n, m, X, Y and R are as defined herein.Type: GrantFiled: December 10, 2002Date of Patent: October 17, 2006Assignee: Temple University - Of The Commonwealth System of Higher EducationInventors: E. Premkumar Reddy, M.V. Ramana Reddy
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Patent number: 7119120Abstract: Disclosed are compounds which have been identified as inhibitors of phosphate transport. Many of the compounds are represented by Structural Formula (I): Ar1—W—X—Y—Ar2; or a pharmaceutically acceptable salt thereof. Ar1 and Ar2 are independently a substituted or unsubstituted aryl group or an optionally substituted five membered or six membered non-aromatic heterocylic group fused to an optionally substituted monocylic aryl group. W and Y are independently a covalent bond or a C1–C3 substituted or unsubstituted alkylene group. X is a heteroatom-containing functional group, an aromatic heterocyclic group, substituted aromatic heterocyclic group, non-aromatic heterocyclic group, substituted non-aromatic heterocyclic group, an olefin group or a substituted olefin group. Also disclosed are methods of treating a subject with a disease associated with hyperphosphatemia, as well as a disease mediated by phosphate-transport function.Type: GrantFiled: December 20, 2002Date of Patent: October 10, 2006Assignee: Genzyme CorporationInventors: Thomas H. Jozefiak, Cecilia M. Bastos, Andrew T. Papoulis, Stephen Randall Holmes-Farley
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Patent number: 7115632Abstract: A sulfonyl aromatic or heteroaromatic ring hydroxamic acid compound that inter alia inhibits matrix metalloprotease activity is disclosed as are a treatment process that comprises administering a contemplated sulfonyl aromatic or heteroaromatic ring hydroxamic acid compound in a MMP enzyme-inhibiting effective amount to a host having a condition associated with pathological matrix metalloprotease activity. A contemplated compound corresponds in structure to the formula wherein W and the R groups are defined elsewhere.Type: GrantFiled: May 11, 2000Date of Patent: October 3, 2006Assignee: G. D. Searle & Co.Inventors: Louis J Bedell, Joseph J McDonald, Thomas E Barta, Daniel P Becker, Rao N Shashidhar, John N Freskos, Brent V Mischke, Daniel P Getman, Gary A DeCrescenzo, Clara I Villamil
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Patent number: 7112611Abstract: The invention relates to ?-amino-N-hydroxy-acetamide derivatives of formula (I), wherein R is di-lower alkyl amino, 1,2,3-triazol-2yl or 1,2,4-triazol-4-yl, m represents an integer from 1 up to and including 10, and n represents an integer from 0 up to and including 10, and salts thereof; to processes for their preparation, pharmaceutical compositions comprising said hydroxamic acid derivatives, the use of such hydroxamic acid derivatives as medicaments, and a method of treating conditions or diseases mediated by matrix-degrading metalloproteinases (MMP's) using said derivatives alone or in combination with one or more other therapeutic agents.Type: GrantFiled: February 8, 2002Date of Patent: September 26, 2006Assignee: Novartis AGInventors: Kenji Hayakawa, Genji Iwasaki, Shinichi Koizumi, Ichiro Umemura
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Patent number: 7109243Abstract: The present invention provides compounds, compositions and methods for the selective inhibition of cathepsin S. In a preferred aspect, cathepsin S is selectively inhibited in the presence of at least one other cathepsin isozyme (e.g., cathespin K). The present invention also provides methods for treating a disease state in a subject by selectively inhibiting cathepsin S.Type: GrantFiled: March 23, 2004Date of Patent: September 19, 2006Assignee: IRM LLCInventors: Hong Liu, David Tully, Robert Epple, Badry Bursulaya, Jennifer Williams, Arnab Chatterjee, Jennifer Leslie Harris, Jun Li
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Patent number: 7101895Abstract: Compounds of formula I: wherein Ar1 and Ar2 are optionally substituted aryl or heteroaryl, L is a bond, ?CH— or —(CHRa)n—, and X is SCN, SR1, S(O)R1, (CRaRb)mSO2R1, SO2N(R2)2, SO2NHCOR1, SO2NHN(R2)2, OSO2N(R2)2, OS(O)N(R2)2, OSO2NHCOR1, COR4, NHCOR1, NHCO2R1, NHCON(R2)2, NHSO2R1 or NHSO2N(R2)2, inhibit the processing of APP by gamma secretase, and hence are useful in treatment of Alzheimer's disease.Type: GrantFiled: October 6, 2003Date of Patent: September 5, 2006Assignee: Merck Sharp & Dohme LimitedInventors: Ian Churcher, Timothy Harrison, Sonia Kerrad, Paul Joseph Oakley, Duncan Edward Shaw, Martin Richard Teall, Susannah Williams
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Patent number: 7094397Abstract: The invention features methods and reagents for the diagnosis, monitoring, and treatment of multiple sclerosis. The invention is based in part on the discovery that Chlamydia is present in patients with multiple sclerosis, and that anti-chlamydial agents improve or sustain neurological function in these patients.Type: GrantFiled: February 17, 2005Date of Patent: August 22, 2006Assignee: Vanderbilt UnversityInventors: Charles W. Stratton, William M. Mitchell, Subramaniam Sriram
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Patent number: 7049468Abstract: Compounds of formula 1 modulate the activity of Rho C: wherein R is a direct bond, lower alkylene, —C(O)NH—, or —NHC(O)—; Ar is aryl or heteroaryl, substituted with R7, R8, R9, and R10, wherein R7, R8, and R9 are each independently H, halo, lower alkyl, OH, lower alkoxy, and R10 is H, halo, lower alkyl, OH, lower alkoxy, or forms a ring with R1; R1 is H, lower alkyl, or forms a ring with R10; R2, R3, R4, R5, and R6 are each independently H, lower alkyl, halo, nitro, OH, lower alkoxy, NH2, lower alkylamino, di(lower alkyl)amino, or two adjacent groups together form a saturated or unsaturated ring; or a pharmaceutically acceptable salt thereof.Type: GrantFiled: November 19, 2002Date of Patent: May 23, 2006Assignee: Iconix Pharmaceuticals, Inc.Inventors: Dongxu Sun, Edward L. Perkins, Stuart Tugendreich
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Patent number: 6967196Abstract: In accordance with the present invention, there is provided a novel class of sulfonamide compounds. Compounds of the invention contain a core sulfonamide group. Variable moieties connected to the sulfur atom and nitrogen atom of the sulfonamide group include substituted or unsubstituted hydrocarbyl moieties, substituted or unsubstituted heterocycle moieties, polycyclic moieties, halogen, alkoxy, ether, ester, amide, sulfonyl, sulfonamidyl, sulfide, carbamate, and the like. Invention compounds are capable of a wide variety of uses. For example sulfonamide compounds can act to modulate production of amyloid ? protein and are useful in the prevention or treatment of a variety of diseases. Pharmaceutical compositions containing invention compounds are also provided. Such compositions have wide utility for the prevention or treatment of a variety of diseases.Type: GrantFiled: February 22, 2000Date of Patent: November 22, 2005Assignees: Bristol-Myers Squibb Company, Merck & Co. Inc.Inventors: David W. Smith, Benito Munoz, Kumar Srinivasan, Carl P. Bergstrom, Prasad V. Chaturvedula, Milind S. Deshpande, Daniel J. Keavy, Wai Yu Lau, Michael F. Parker, Charles P. Sloan, Owen B. Wallace, Henry Hui Wang
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Patent number: 6965048Abstract: The present invention relates to compounds of formula (I) wherein R1, R2, R3, R4, X, W, m and n are as defined hereinabove. The compounds are useful for the treatment and/or prophylaxis of diseases which are associated with 2,3-oxidosqualene-lanosterol cyclase such as hypercholesterolemia, hyperlipemia, arteriosclerosis, vascular diseases, mycoses, parasite infections, gallstones, tumors and/or hyperproliferative disorders, and treatment and/or prophylaxis of impaired glucose tolerance and diabetes.Type: GrantFiled: July 1, 2004Date of Patent: November 15, 2005Assignee: Hoffmann-La Roche Inc.Inventors: Jean Ackermann, Johannes Aebi, Henrietta Dehmlow, Olivier Morand, Narendra Panday
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Patent number: 6963010Abstract: The disclosed invention provides new polyamine analogs and derivatives containing a hydrophobic region and a polyamine region as well as methods and compositions for their use.Type: GrantFiled: January 8, 2002Date of Patent: November 8, 2005Assignee: MediQuest Therapeutics, Inc.Inventors: Mark R. Burns, Gerard F. Graminski
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Patent number: 6946485Abstract: Disclosed are methods for inhibiting Ras activity such as cell proliferation associated with vascular injury such as post-angioplasty restenosis and atherosclerosis. Preferred Ras antagonists are S-trans-trans farnesylthiosalicylic acid (FTS) and structurally related compounds (or analogs) thereof.Type: GrantFiled: April 22, 2003Date of Patent: September 20, 2005Assignee: Ramot at Tel Aviv University, Ltd.Inventors: Yoel Kloog, Gad Keren, Jakob George
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Patent number: 6943170Abstract: This invention relates generally to N-cycloalkylglycines of the Formula (I): or a stereoisomeric form, a mixture of stereoisomeric forms, or a pharmaceutically acceptable salt thereof, which are useful as HIV protease inhibitors, pharmaceutical compositions and diagnostic kits including the same, methods for using the same for treating viral infection or an assay standards or reagents, and intermediates and processes for making the same.Type: GrantFiled: October 30, 2003Date of Patent: September 13, 2005Assignee: Bristol-Myers Squibb CompanyInventor: David J. Carini
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Patent number: 6927224Abstract: The present invention provides, inter alia, triphenylethylene derivatives, such as, 3-{4-[6-(3-Methoxy-phenyl)-8,9-dihydro-7H-benzocyclohepten-5-yl]-phenyl}-acrylic acid, as selective estrogen receptor modulators. Also provided are methods for the treatment and/or prevention of estrogen stimulated diseases in mammals including breast, uterine, ovarian, prostrate and colon cancer, osteoporosis, cardiovascular disease, and benign proliferative disorders, as well as pharmaceutical compositions of the compounds of the present invention.Type: GrantFiled: August 9, 2002Date of Patent: August 9, 2005Assignee: Bristol Myers Squibb CompanyInventors: Robert F. Kaltenbach, Simon P. Robinson, George L. Trainor
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Patent number: 6919375Abstract: Compounds having a metalloproteinase inhibitory activity, represented by the formula (I), its optically active isomers, their pharmaceutically acceptable salts, or hydrates thereof.Type: GrantFiled: July 22, 1998Date of Patent: July 19, 2005Assignee: Shionogi & Co., Ltd.Inventors: Fumihiko Wantanabe, Hiroshige Tsuzuki, Mitsuaki Ohtani
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Patent number: RE39682Abstract: Novel farnesyl derivatives which are inhibitors of the prenylated protein methyltransferase enzyme, and useful as anti-cancer drugs, have the following formula: wherein R1represents farnesyl, geranyl or geranyl-geranyl; Z represents C—R6 or N; R2 represents H, CN, the groups COOR7, SO3R7, CONR7R8 and SO2NR7R7, wherein R7 and R8 are each independently hydrogen, alkyl, alkenyl, and the groups COOM and SO3M, wherein M is a cation; R3, R4, R5 and R6 are each independently hydrogen, carboxyl, alkyl, alkenyl, aminoalkyl, nitroalkyl, nitro, halo, amino, mono- or di-alkylamino, mercapto, mercaptoalkyl, azido, or thiocyanato; X represents O, S, SO, SO2, NH or Se; and the quaternary ammonium salts and N-oxides of the compounds of formula I wherein Z is N.Type: GrantFiled: March 30, 2005Date of Patent: June 5, 2007Assignee: Ramot at Tel Aviv University Ltd.Inventor: Yoel Kloog