Fully Saturated Quinolines Patents (Class 546/164)
  • Patent number: 8993567
    Abstract: Novel cyclic compounds and salts thereof, pharmaceutical compositions containing such compounds, and methods of using such compounds in the treatment of protein tyrosine kinase-associated disorders such as immunologic and oncologic disorders.
    Type: Grant
    Filed: March 27, 2014
    Date of Patent: March 31, 2015
    Assignee: Bristol-Myers Squibb Company
    Inventors: Jagabandhu Das, Ramesh Padmanabha, Ping Chen, Derek Norris, Arthur M. P. Doweyko, Joel C. Barrish, John Wityak
  • Patent number: 8937184
    Abstract: The invention relates to a group of 1H-imidazole derivatives which are modulators of cannabinoid CB2 receptors, to methods for the preparation of these compounds, to novel intermediates useful for the synthesis of said imidazole derivatives, to methods for the preparation of these intermediates, to pharmaceutical compositions containing one or more of these 1H-imidazole derivatives as active ingredient, as well as to the use of these pharmaceutical compositions for the treatment of disorders in which cannabinoid CB2 receptors are involved. The compounds have the general formula (I) wherein R1-R4 have the meanings given in the specification.
    Type: Grant
    Filed: February 14, 2006
    Date of Patent: January 20, 2015
    Assignee: Abbvie B.V.
    Inventors: Josephus H. M. Lange, Herman H. Van Stuivenberg, Bernard J. Van Vliet
  • Publication number: 20140206691
    Abstract: Novel cyclic compounds and salts thereof, pharmaceutical compositions containing such compounds, and methods of using such compounds in the treatment of protein tyrosine kinase-associated disorders such as immunologic and oncologic disorders.
    Type: Application
    Filed: March 27, 2014
    Publication date: July 24, 2014
    Inventors: Jagabandhu Das, Ramesh Padmanabha, Ping Chen, Derek Norris, Arthur M.P. Doweyko, Joel C. Barrish, John Wityak
  • Patent number: 8741924
    Abstract: Small molecule compounds are provided for treating lupus as are methods of treating lupus using these compounds.
    Type: Grant
    Filed: May 6, 2011
    Date of Patent: June 3, 2014
    Assignee: The Feinstein Institute for Medical Research
    Inventors: Yousef Al-Abed, Betty A. Diamond
  • Patent number: 8546575
    Abstract: The present invention relates to NIP thiazole derivatives of formula (I) as selective inhibitors of the enzyme 11-beta-hydroxysteroid dehydrogenase type 1 (11-?-HSD-1) and the use of such compounds for the treatment and prevention of metabolic syndrome, diabetes, insulin resistance, obesity, lipid disorders, glaucoma, osteoporosis, cognitive disorders, anxiety, depression, immune disorders, hypertension and other diseases and conditions.
    Type: Grant
    Filed: April 8, 2009
    Date of Patent: October 1, 2013
    Assignee: Merck Patent GmbH
    Inventors: Caroline Leriche, Denis Carniato, Didier Roche, Christine Charon, Liliane Doare
  • Patent number: 8546427
    Abstract: The present invention relates to compounds according to formula (I) and pharmaceutically acceptable salts or esters thereof, wherein R1 to R7 have the significance given herein. The compounds are activators of AMP-activated protein kinase (AMPK) and are useful in the treatment or prophylaxis of diseases that are related to AMPK regulation, such as obesity, dyslipidemia, hyperglycemia, type 1 or type 2 diabetes and cancers.
    Type: Grant
    Filed: October 13, 2011
    Date of Patent: October 1, 2013
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Lichun Feng, Mengwei Huang, Yongfu Liu, Guolong Wu, Mingwei Zhou
  • Patent number: 8541595
    Abstract: The present invention is directed to imidazoisoindole compounds which are antagonists of neuropeptide S receptors, and which are useful in the treatment or prevention of neurological and psychiatric disorders and diseases in which the neuropeptide S receptor is involved. 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 neuropeptide S receptor is involved.
    Type: Grant
    Filed: November 3, 2009
    Date of Patent: September 24, 2013
    Assignee: Merch Sharp & Dohme Corp.
    Inventors: Peter J. Manley, Kausik K Nanda, B. Wesley Trotter
  • Patent number: 8530137
    Abstract: The present invention provides a photoresist composition having a sulfonium salt comprising an anion represented by the formula (IA): wherein R1 and R2 independently represent a hydrogen atom, a C1-C12 aliphatic hydrocarbon group, a C3-C20 saturated cyclic hydrocarbon group, a C6-C20 aromatic hydrocarbon group or a C7-C21 aralkyl group, and the aliphatic hydrocarbon group, the saturated cyclic hydrocarbon group, the aromatic hydrocarbon group and the aralkyl group can have one or more substituents selected from the group consisting of a hydroxyl group, a cyano group, a fluorine atom, a trifluoromethyl group and a nitro group, and one or more —CH2— in the aliphatic hydrocarbon group can be replaced by —O— or —CO—, or R1 and R2 are bonded each other to form a C4-C20 nitrogen-containing ring together with the nitrogen atom to which they are bonded, an acrylic resin having an acid-labile group and being insoluble or poorly soluble in an aqueous alkali solution but becoming soluble in an aqueous alkali solutio
    Type: Grant
    Filed: February 11, 2011
    Date of Patent: September 10, 2013
    Assignee: Sumitomo Chemical Company, Limited
    Inventors: Tatsuro Masuyama, Satoshi Yamaguchi
  • Patent number: 8476443
    Abstract: The present invention provides dyes and labeled reagents that may be used in the detection or quantification of desirable target molecules, such as proteins, nucleic acids and cellular organelles. Dyes are provided that may be used free in solution where the binding of the dye to the target molecule provides signal generation. Dyes provided in this invention can comprise reactive groups that may be used to attach the dyes to probes that will bind to desirable target molecules. The novel dyes of the present invention have been substituted with specific groups to provide beneficial properties.
    Type: Grant
    Filed: January 3, 2013
    Date of Patent: July 2, 2013
    Assignee: Enzo Life Sciences, Inc.
    Inventors: Praveen Pande, Hilary J. Cox, Yuejun Xiang, Wayne Forrest Patton
  • Patent number: 8377698
    Abstract: Disclosed are a novel 8-hydroxyquinoline acetamide compound, an 8-hydroxyquinoline thioamide and use thereof. More specifically, disclosed are a novel 8-hydroxyquinoline thioamide compound suitable for use as a selective chemodosimeter that shows considerably high detection sensitivity to mercury ions, an 8-hydroxyquinoline acetamide compound as an intermediate thereof, preparation thereof, and a chemodosimeter for mercury ion-selective detection, the chemodosimeter comprising the 8-hydroxyquinoline thioamide compound. The compounds as disclosed herein exhibit considerably effective fluorescence specificity of an off-on type, detect a micromole of mercury ions from chemical and biological aqueous systems, and allow 100% desulfurization within 5 minutes, thus being considerably useful in the chemical industry.
    Type: Grant
    Filed: September 24, 2011
    Date of Patent: February 19, 2013
    Assignees: Samsung Electronics Co., Ltd., Seoul National University Industry Foundation, Chung-Ang University Inudstry-Academy Cooperation Foundation
    Inventors: Suk Kyu Chang, Ki Cheol Song, Jun Soo Kim, Sang Mi Park, Sang Doo Ahn, Jae Young Sung
  • Patent number: 8362008
    Abstract: The present invention pertains generally to the field of therapeutic compounds. More specifically the present invention pertains to certain amido-thiophene compounds that, inter alia, inhibit 11?-hydroxysteroid dehydrogenase type 1 (11?-HSD1). The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo, to inhibit 11?-hydroxysteroid dehydrogenase type 1; to treat disorders that are ameliorated by the inhibition of 11?-hydroxysteroid dehydrogenase type 1; to treat the metabolic syndrome, which includes disorders such as type 2 diabetes and obesity, and associated disorders including insulin resistance, hypertension, lipid disorders and cardiovascular disorders such as ischaemic (coronary) heart disease; to treat CNS disorders such as mild cognitive impairment and early dementia, including Alzheimer's disease; etc.
    Type: Grant
    Filed: December 11, 2008
    Date of Patent: January 29, 2013
    Assignee: The University Of Edinburgh
    Inventors: Scott Peter Webster, Jonathan Robert Seckl, Brian Robert Walker, Peter Ward, Thomas David Pallin, Hazel Joan Dyke, Trevor Robert Perrior
  • Publication number: 20120309751
    Abstract: New tertiary 8-hydroxyquinoline-7-carboxamide derivatives of general formula (I) and pharmaceutically acceptable salts thereof are disclosed. These compounds are useful as antifungal agents. Specifically, these compounds were tested against Tricophyton Rubrum, Tricophyton Mentagrophytes, Aspergillus Niger and Scopulariopsis Brevicaulis. These compounds are also active against Candida species such as Candida Albicans and Candida Glabrata.
    Type: Application
    Filed: December 28, 2010
    Publication date: December 6, 2012
    Applicant: POLICHEM SA
    Inventors: Stefania Gagliardi, Simone Del Sordo, Federico Mailland, Michela Legora
  • Patent number: 8299063
    Abstract: The present invention pertains generally to the field of therapeutic compounds. More specifically the present invention pertains to certain amido-thiophene compounds that, inter alia, inhibit 11?-hydroxysteroid dehydrogenase type 1 (11?-HSD1). The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo, to inhibit 11?-hydroxysteroid dehydrogenase type 1; to treat disorders that are ameliorated by the inhibition of 11?-hydroxysteroid dehydrogenase type 1; to treat the metabolic syndrome, which includes disorders such as type 2 diabetes and obesity, and associated disorders including insulin resistance, hypertension, lipid disorders and cardiovascular disorders such as ischaemic (coronary) heart disease; to treat CNS disorders such as mild cognitive impairment and early dementia, including Alzheimer's disease; etc.
    Type: Grant
    Filed: March 13, 2009
    Date of Patent: October 30, 2012
    Assignee: The University of Edinburgh
    Inventors: Scott Peter Webster, Jonathan Robert Seckl, Brian Robert Walker, Peter Ward, Thomas David Pallin, Hazel Joan Dyke, Trevor Robert Perrior
  • Publication number: 20120095046
    Abstract: The present invention pertains generally to the field of therapeutic compounds. More specifically the present invention pertains to certain amido-isothiazole compounds that, inter alia, inhibit 11?-hydroxysteroid dehydrogenase type 1 (11?-HSD1). The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo, to inhibit 11?-hydroxysteroid dehydrogenase type 1; to treat disorders that are ameliorated by the inhibition of 11?-hydroxysteroid dehydrogenase type 1; to treat the metabolic syndrome, which includes disorders such as type 2 diabetes and obesity, and associated disorders including insulin resistance, hypertension, lipid disorders and cardiovascular disorders such as ischaemic (coronary) heart disease; to treat CNS disorders such as mild cognitive impairment and early dementia, including Alzheimer's disease; etc.
    Type: Application
    Filed: June 14, 2010
    Publication date: April 19, 2012
    Applicant: THE UNIVERSITY OF EDINBURGH
    Inventors: Scott Peter Webster, Jonathan Robert Seckl, Brian Robert Walker, Peter Ward, Thomas David Pallin, Hazel Joan Dyke, Trevor Robert Perrior
  • Publication number: 20120071466
    Abstract: The compounds of formula (I) are derived from perhydroquinoline and perhydroisoquinoline and are useful as active pharmaceutical ingredients for the prophylaxis or treatment of diseases caused by 11-beta-hydroxysteroid dehydrogenase type I (11-beta-HSD1) enzyme-associated disorders, such as glaucoma, elevated ocular pressure, metabolic disorders, obesity, metabolic syndrome, dyslipidemia, hypertension, diabetes, atherosclerosis, Cushing's syndrome, psoriasis, rheumatoid arthritis, cognitive disorders, Alzheimer's disease or neurodegeneration.
    Type: Application
    Filed: June 4, 2010
    Publication date: March 22, 2012
    Inventors: Juan Lorenzo Catena Ruiz, Carme Serra Comas, Oscar Rey Puiggros, Albert Antolin Hernandez, Esther Monlleomas
  • Publication number: 20110312949
    Abstract: The use of substituted amides for modulating the activity of 11?-hydroxysteroid dehydrogenase type 1 (11?HSD1) and the use of these compounds as pharmaceutical compositions, are described. Also a novel class of substituted amides, their use in therapy, pharmaceutical compositions comprising the compounds, as well as their use in the manufacture of medicaments are described. The present compounds are modulators and more specifically inhibitors of the activity of 11?HSD1 and may be useful in the treatment, prevention and/or prophylaxis of a range of medical disorders where a decreased intracellular concentration of active glucocorticoid is desirable.
    Type: Application
    Filed: August 30, 2011
    Publication date: December 22, 2011
    Applicant: HIGH POINT PHARMACEUTICALS, LLC
    Inventors: John Paul Kilburn, Henrik Sune Andersen, Gita Camilla Tejlgaard Kampen, Soren Ebdrup
  • Publication number: 20110288111
    Abstract: Provided are compounds that are capable of modulating the activity of the influenza A virus via interaction with the M2 transmembrane protein. Also provided are methods for treating an influenza A-affected disease state or infection comprising administering a composition comprising one or more compounds that have been identified as being capable of interaction with the M2 protein.
    Type: Application
    Filed: August 21, 2009
    Publication date: November 24, 2011
    Applicant: The Trustees of the University of Pennsylvania
    Inventors: William F. DeGrado, Jun Wang
  • Patent number: 8058074
    Abstract: Disclosed are a novel 8-hydroxyquinoline acetamide compound, an 8-hydroxyquinoline thioamide and use thereof. More specifically, disclosed are a novel 8-hydroxyquinoline thioamide compound suitable for use as a selective chemodosimeter that shows considerably high detection sensitivity to mercury ions, an 8-hydroxyquinoline acetamide compound as an intermediate thereof, preparation thereof, and a chemodosimeter for mercury ion-selective detection, the chemodosimeter comprising the 8-hydroxyquinoline thioamide compound. The compounds as disclosed herein exhibit considerably effective fluorescence specificity of an off-on type, detect a micromole of mercury ions from chemical and biological aqueous systems, and allow 100% desulfurization within 5 minutes, thus being considerably useful in the chemical industry.
    Type: Grant
    Filed: July 6, 2007
    Date of Patent: November 15, 2011
    Assignees: Samsung Electronics Co., Ltd., Seoul National University Industry Foundation, Chung-Ang University Industry-Academy Cooperation Foundation
    Inventors: Suk Kyu Chang, Ki Cheol Song, Jun Soo Kim, Sang Mi Park, Sang Doo Ahn, Jae Young Sung
  • Publication number: 20110152318
    Abstract: This present invention relates to novel compounds, isomer thereof or pharmaceutically acceptable salts thereof as vanilloid receptor (Vanilloid Receptor 1; VR1; TRPV1) antagonist; and a pharmaceutical composition containing the same. The present invention provides a pharmaceutical composition for preventing or treating a disease such as pain, migraine, arthralgia, neuralgia, neuropathies, nerve injury, skin disorder, urinary bladder hypersensitiveness, irritable bowel syndrome, fecal urgency, a respiratory disorder, irritation of skin, eye or mucous membrane, stomach-duodenal ulcer, inflammatory diseases, ear disease, heart disease and so on.
    Type: Application
    Filed: July 2, 2009
    Publication date: June 23, 2011
    Applicant: Amorepacific Corporation
    Inventors: Byoung Young Woo, Sun-Young Kim, Yeonjoon Kim, Song Seok Shin, Jin Kwan Kim, Ki-Wha Lee, Dong Hyun Kim, Kyung Min Lim, Joo-Hyun Moh, Yeon Su Jeong, Jin Kyu Choi, Hyun Ju Koh, Jeongho Lee, Hyuk Kim, Jeong Hoon Yoon, Funan Li, Jee-Suk Kim, Young-Ger Suh
  • Publication number: 20110117057
    Abstract: The present invention discloses novel compounds which have HCV protease inhibitory activity as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising such compounds as well as methods of using them to treat disorders associated with the HCV protease.
    Type: Application
    Filed: December 20, 2010
    Publication date: May 19, 2011
    Applicants: SCHERING CORPORATION, DENDREON CORPORATION
    Inventors: Anil K. Saksena, Viyyoor Moopil Girijavallabhan, Raymond G. Lovey, Edwin Jao, Frank Bennett, Jinping L. McCormick, Haiyan Wang, Russell E. Pike, Stephane L. Bogen, Tin-Yau Chan, Yi-Tsung Liu, Zhaoning Zhu, F. George Njoroge, Ashok Arasappan, Tejal Parekh, Ashit K. Ganguly, Kevin X. Chen, Srikanth Venkatraman, Henry A. Vaccaro, Patrick A. Pinto, Bama Santhanam, Scott Jeffrey Kemp, Odile Esther Levy, Marguerita Lim-Wilby, Susan Y. Tamura, Wanli Wu, Siska Hendrata, Yuhua Huang
  • Patent number: 7943605
    Abstract: The present invention relates to compounds of formula (I) comprising a lactam or a lactam derivative moiety, processes for preparing them, pharmaceutical compositions comprising said compounds and their uses as pharmaceuticals.
    Type: Grant
    Filed: October 25, 2006
    Date of Patent: May 17, 2011
    Assignee: UCB Pharma S.A.
    Inventors: Sylvain Celanire, Luc Quere, Frédéric Denonne, Laurent Provins
  • Publication number: 20110059950
    Abstract: Viruses, and particularly RNA viruses, have high mutation rates. Hence, antiviral agents that have been developed to date targeting protease or reverse transcriptase of viruses have quickly lost their effectiveness and resistant viruses have emerged. Also, in recent years, viral diseases caused by various new viruses such as SARS, avian influenza, and the hepatitis C have become social menaces. Therefore, the development of a novel antiviral agent that can cope with a virus resistant to an existing drug or a new virus and has a wide range of applications has been demanded. The present invention provides a novel anti-RNA viral agent and a method for use thereof. The present invention further provides an anti-RNA viral agent that is also effective against a new virus or a drug-resistant virus, and a method for use thereof.
    Type: Application
    Filed: February 4, 2009
    Publication date: March 10, 2011
    Applicant: KinoPharma, Inc.
    Inventors: Hiroshi Onogi, Masatoshi Hagiwara, Masaaki Suzuki, Hiroko Koyama, Takamitsu Hosoya, Toshiyuki Hiramatsu
  • Publication number: 20110060007
    Abstract: The present invention relates to NIP thiazole derivatives of formula (I) as selective inhibitors of the enzyme 11-beta-hydroxysteroid dehydrogenase type 1 (11-?-HSD-1) and the use of such compounds for the treatment and prevention of metabolic syndrome, diabetes, insulin resistance, obesity, lipid disorders, glaucoma, osteoporosis, cognitive disorders, anxiety, depression, immune disorders, hypertension and other diseases and conditions.
    Type: Application
    Filed: April 8, 2009
    Publication date: March 10, 2011
    Applicant: Merck Patent Gesellschaft Mit Beschrankter Haftling
    Inventors: Caroline Leriche, Denis Carniato, Didier Roche, Christine Charon, Liliane Doare
  • Publication number: 20100292215
    Abstract: A novel class of compounds of the general formula (I), their use in therapy, pharmaceutical compositions comprising the compounds, as well as their use in the manufacture of medicaments are described. The present compounds modulate the activity of 11?-hydroxy-steroid dehydrogenase type 1 (11?HSD1) and are accordingly useful in the treatment of diseases in which such a modulation is beneficial, e.g. the metabolic syndrome.
    Type: Application
    Filed: March 27, 2007
    Publication date: November 18, 2010
    Applicant: HIGH POINT PHARMACEUTICALS, LLC
    Inventors: Soren Ebdrup, Henrik Sune Andersen
  • Publication number: 20100280034
    Abstract: The present invention relates to the use of compounds of the general Formula (XIII): wherein A7 is C?O, C?S, SO2, CH—OR13, C?NR12, or CH2—CHOR13; A8 is C(R14)2, O, S, or NR12; A9 is C?O, C?S, SO2, CH—OR13, C?NR12, or CH2—CHOR13; m is 0, or 1 q is 0, or 1 r is 0, or 1 R12 is H, CH3, CH2—CH3, C6H5, OCH3, OCH2—CH3, OH, or SH; R13 is H, CH3, or CH2—CH3; R14 is H, alkyl, alkoxy, OH, or SH;
    Type: Application
    Filed: December 28, 2007
    Publication date: November 4, 2010
    Inventors: Aldo Ammendola, Katharina Aulinger-Fuchs, Astrid Gotschlich, Bernd Kramer, Martin Lang, Wael Saeb, Udo Sinks, Andreas Wuzik
  • Publication number: 20100267697
    Abstract: The present teachings provide compounds of Formula (I) and pharmaceutically acceptable salts, hydrates, and esters thereof, wherein Ar, R1, R2, R3, p, and X are defined herein. The present teachings also provide processes for producing said compounds and their pharmaceutically acceptable salts, hydrates and esters, and methods of treating a pathological condition or disorder, or alleviating a symptom thereof, using said compounds including their pharmaceutically acceptable salts, hydrates and esters. The compounds can be useful in modulating ion channel activity including treating a variety of conditions associated with the abnormal modulation of one or more voltage-gated calcium channels.
    Type: Application
    Filed: December 11, 2007
    Publication date: October 21, 2010
    Applicant: Wyeth
    Inventors: Vincent P. Galullo, Robert Zelle, Danielle Soenen, Christopher Todd Baker, Paul Will, Hormoz Mazdiyasni, Jinsong Guo, Andrew Fensome, Jeffrey Curtis Kern, William Jay Moore, Edward George Melenski, Justin Kaplan
  • Publication number: 20100267696
    Abstract: The present invention pertains generally to the field of therapeutic compounds. More specifically the present invention pertains to certain amido-thiophene compounds that, inter alia, inhibit 11?-hydroxysteroid dehydrogenase type 1 (11?-HSD1). The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo, to inhibit 11?-hydroxysteroid dehydrogenase type 1; to treat disorders that are ameliorated by the inhibition of 11?-hydroxysteroid dehydrogenase type 1; to treat the metabolic syndrome, which includes disorders such as type 2 diabetes and obesity, and associated disorders including insulin resistance, hypertension, lipid disorders and cardiovascular disorders such as ischaemic (coronary) heart disease; to treat CNS disorders such as mild cognitive impairment and early dementia, including Alzheimer's disease; etc.
    Type: Application
    Filed: December 11, 2008
    Publication date: October 21, 2010
    Applicant: THE UNIVERSITY OF EDINBURGH
    Inventors: Scott Peter Webster, Jonathan Robert Seckl, Brian Robert Walker, Peter Ward, Thomas David Pallin, Hazel Joan Dyke, Trevor Robert Perrior
  • Patent number: 7807694
    Abstract: Compounds which modulate chemokine receptor activities are disclosed. These compounds are preferably tertiary amines comprising tetrahydroquinoline and benzimidazole.
    Type: Grant
    Filed: July 14, 2006
    Date of Patent: October 5, 2010
    Assignee: Genzyme Corporation
    Inventors: Gary Bridger, Renato Skerlj, Al Kaller, Curtis Harwig, David Bogucki, Trevor R. Wilson, Jason Crawford, Ernest J. McEachern, Bem Atsma, Siqiao Nan, Yuanxi Zhou, Dominique Schols, Christopher Dennis Smith, Maria Rosaria Di Fluri
  • Publication number: 20100249097
    Abstract: The invention relates to substituted tetrahydronaphthalenes and derivatives thereof, and also to the physiologically compatible salts and physiologically functional derivatives thereof, to preparation thereof, to medicaments comprising at least one inventive substituted tetrahydronaphthalene or derivative thereof, and to the use of the inventive substituted tetrahydronaphthalenes and derivatives thereof as medicaments.
    Type: Application
    Filed: February 12, 2010
    Publication date: September 30, 2010
    Applicant: SANOFI-AVENTIS
    Inventors: Lothar SCHWINK, Siegfried STENGELIN, Matthias GOSSEL, Torsten HAACK, Petra LENNIG
  • Publication number: 20100197662
    Abstract: Disclosed is a compound useful as a type I 11?hydroxysteroid dehydrogenase inhibitor. A compound represented by the formula: a pharmaceutically acceptable salt or solvate thereof, wherein R1 is optionally substituted cycloalkyl, optionally substituted cycloalkenyl or the like, One of R2 and R3 is a group of the formula: —C(?O)—Y—R4, wherein Y is —NR9— or the like, R4 is optionally substituted cycloalkyl or the like, R9 is hydrogen or optionally substituted alkyl, W is optionally substituted alkylene, The other is a group of the formula: —V—R5, wherein V is a bond, —O— or the like, R6 is hydrogen or optionally substituted alkyl, R5 is hydrogen, optionally substituted alkyl or the like, X is a bond, —S—, —SO— or the like, U is a bond or optionally substituted alkylene, R7 is hydrogen or optionally substituted alkyl, Z is —S—, —O— or —NR8—, R8 is hydrogen, optionally substituted alkyl or the like.
    Type: Application
    Filed: June 6, 2006
    Publication date: August 5, 2010
    Applicant: Shionogi & Co., Ltd.
    Inventors: Tomoyuki Ogawa, Noriyuki Kurose, Satoru Tanaka, Koichi Nishi
  • Publication number: 20100152236
    Abstract: A compound represented by the formula (I) wherein ring A is a 5- to 8-membered ring optionally having further substituent(s) other than R6, R7 and R8, R1 is an electron-withdrawing group, R2, R3, R4 and R5 are each independently a hydrogen atom, a halogen atom, a group bonded via a carbon atom, a group bonded via a nitrogen atom, a group bonded via an oxygen atom or a group bonded via a sulfur atom, R6 is a halogen atom, a group bonded via a carbon atom, a group bonded via a nitrogen atom, a group bonded via an oxygen atom or a group bonded via a sulfur atom, R7 is a cyano group, a nitro group, an acyl group optionally having substituent(s), an optionally esterified or amidated carboxyl group or a hydrocarbon group optionally having substituent(s), or R6 and R7 optionally form, together with the carbon atom bonded thereto, a ring optionally having substituent(s), and R8 is a hydrogen atom, a halogen atom, a group bonded via a carbon atom, a group bonded via a nitrogen atom, a group bonded via an oxyg
    Type: Application
    Filed: August 1, 2006
    Publication date: June 17, 2010
    Applicant: Takeda Pharmaceutical Company Limited
    Inventors: Satoshi Yamamoto, Atsushi Hasuoka
  • Publication number: 20090306048
    Abstract: A novel class of compounds of the general formula (I), their use in therapy, pharmaceutical compositions comprising the compounds, as well as their use in the manufacture of medicaments are described. The present compounds modulate the activity of 11?-hydroxysteroid dehydrogenase type 1 (11?HSD1) and are accordingly useful in the treatment of diseases in which such a modulation is beneficial, e.g. the metabolic syndrome.
    Type: Application
    Filed: June 14, 2007
    Publication date: December 10, 2009
    Inventors: John Paul Kilburn, Gita Camilla Tejlgaard Kampen, Henrik Sune Andersen
  • Publication number: 20090264405
    Abstract: Compounds of Formula I, including pharmaceutically acceptable salts of the compounds, are CETP inhibitors, and are useful for raising HDL-cholesterol, reducing LDL-cholesterol, and for treating or preventing atherosclerosis.
    Type: Application
    Filed: October 30, 2006
    Publication date: October 22, 2009
    Inventors: Amjad Ali, Julianne A. Hunt, Florida Kallashi, Jennifer Kowalchick, Dooseop Kim, Cameron J. Smith, Peter J. Sinclair, Ramzi F. Sweis, Gayle E. Taylor, Christopher F. Thompson, Liya Chen, Nazia Quraishi
  • Publication number: 20090218039
    Abstract: An dye compound of the following formula (1): wherein D represents a substituted or unsubstituted aryl group, or a substituted or unsubstituted heterocyclic group; L represents ?CR2—, ?N—, or ?N—NH—; R1 represents a monovalent substituent; R2 represents a hydrogen atom or a cyano group; n indicates an integer of from 0 to 4; when n is 2 or more, then plural R1's may be the same or different.
    Type: Application
    Filed: February 27, 2009
    Publication date: September 3, 2009
    Applicant: FUJIFILM Corporation
    Inventors: Yoshihiko FUJIE, Tetsuya WATANABE, Hisashi MIKOSHIBA
  • Patent number: 7432282
    Abstract: Novel indole derivatives of the formula (I), in which X, Y, R1, R1?, m and n have the meanings indicated in Patent Claim 1, have a strong affinity to the 5-HT1A and in some cases to the 5-HT1D receptors.
    Type: Grant
    Filed: October 30, 2003
    Date of Patent: October 7, 2008
    Assignee: Merck Patent Gesellschaft mit beschrankter Haftung
    Inventors: Günter Hölzemann, Kai Schiemann, Timo Heinrich, Henning Böttcher, Joachim Leibrock, Christoph van Amsterdam, Gerd Bartoszyk, Christoph Seyfried
  • Patent number: 7335677
    Abstract: Novel compounds that are inhibitors of one or most post-proline cleaving proteases, e.g. dipeptidyl peptidase IV, according to general formula (1). R1 is H or CN, X1 is O, S, CH2, CHF, CF2, CH(CH3), C(CH3)2 or CH(CN), and b is 1 or 2. G1 is H or a group according to the formula —CH2—X2—(CH2)a-G3 and G2 is H or a group according to the formula —CH2—(CH29a-G3, provided that one of G1 and G2 is H and the other is not H. X2 is O, S, or CH2, and a is 0, 1 or 2, provided that when a is 1 then X2 is CH2. G3 is a group according to one of general formulae 2-4, where the variables have meaning given in the description. The compounds are useful in the treatment of i.a.
    Type: Grant
    Filed: October 23, 2002
    Date of Patent: February 26, 2008
    Assignee: Ferring B.V.
    Inventors: David M. Evans, Doreen M. Ashworth
  • Patent number: 7312222
    Abstract: The present application describes modulators of CCR3 of formula (I): or pharmaceutically acceptable salt forms thereof, useful for the prevention of asthma and other allergic diseases.
    Type: Grant
    Filed: March 25, 2004
    Date of Patent: December 25, 2007
    Assignee: Bristol-Myers Squibb Pharma Company
    Inventors: Soo S. Ko, George V. Delucca, John V. Duncia, Joseph B. Santella, III, Dean A. Wacker
  • Patent number: 7273936
    Abstract: Novel oxazole and thiazole compounds, including derivatives thereof, to intermediates for their preparation, to pharmaceutical compositions containing them and to their medicinal use are described. The compounds of the present invention are potent inhibitors of transforming growth factor (“TGF”)-? signaling pathway. They are useful in the treatment of various TGF-related disease states including, for example, cancer and fibrotic diseases.
    Type: Grant
    Filed: September 17, 2003
    Date of Patent: September 25, 2007
    Assignee: Pfizer Inc.
    Inventors: Michael J. Munchhof, Laura C. Blumberg
  • Patent number: 7214714
    Abstract: 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: Grant
    Filed: April 26, 2002
    Date of Patent: May 8, 2007
    Assignee: Taisho Pharmaceutical Co. Ltd.
    Inventors: Masakazu Sato, Noriyuki Miyata, Takaaki Ishii, Yuko Matsunaga, Hideaki Amada
  • Patent number: 7189758
    Abstract: A compound of Formula (I) wherein R1, R2, R3, R4, R5, and R6 are as defined herein, or a tautomer, prodrug, solvate, or salt thereof; pharmaceutical compositions containing such compounds, and methods of modulating the glucocorticoid receptor function and methods of treating disease-states or conditions mediated by the glucocorticoid receptor function or characterized by inflammatory, allergic, or proliferative processes in a patient using these compounds.
    Type: Grant
    Filed: October 5, 2005
    Date of Patent: March 13, 2007
    Assignee: Boehringer Ingelheim Pharmaceuticals, Inc.
    Inventors: Rajashekhar Betageri, David Thomson, Yan Zhang, Renee Michele Zindell
  • Patent number: 7145021
    Abstract: The subject invention provides compounds having the structure: wherein R1 is H, OH, a photoactivatable moiety, a fluorescent moiety, or a radioactive moiety; R2 is H, OH, a photoactivatable moiety, a fluorescent-moiety, or a radioactive moiety; R3 is H or OH; R4 is H, OH, a photoactivatable moiety, a fluorescent moiety, or a radioactive moiety; and wherein at least one of R1, R2, R3, or R4 is a photoactivatable moiety, a fluorescent moiety, or a radioactive moiety, or an optically pure enantiomer of the compound or wherein R1 is H or OH; R2 is H, OH, halogen, unsubstituted or substituted, straight or branched (C1–C5) alkyl group, (C2–C5) alkenyl, or a (C2–C5) alkynyl, (C1–C5) alkoxy, (C2–C5) alkenyloxy, or (C2–C5) alkynyloxy, —N3, —COR5, —CONR5R6, —CO2R5, —OCOR5, —NH(OH), —NR5R6, —NHCOR5, —N(OH)COR5, —CH2OR5, —OCH2CO2R5, —CH2SR5, —CH2NR5R6, —SR5, —OSR5, or —NR5SO2R6, where R5 and R6 are each independently hydrogen, substituted or unsubstituted (C1–C5) alkyl, (C2–C5) alkenyl, or (C2–C5) alkynyl, or a cyclo
    Type: Grant
    Filed: March 28, 2003
    Date of Patent: December 5, 2006
    Assignee: The Trustees of Columbia University in the City of New York
    Inventors: Kristian Stromgaard, Makiko Suehiro, Koji Nakanishi, Stine B. Vogensen
  • Patent number: 7084155
    Abstract: Novel compounds that are useful for targeting chemokine receptors are disclosed. These compounds are complex tertiary amines.
    Type: Grant
    Filed: June 1, 2004
    Date of Patent: August 1, 2006
    Assignee: AnorMED
    Inventors: Gary Bridger, Renato Skerlj, Al Kaller, Curtis Harwig, David Bogucki, Trevor R. Wilson, Jason Crawford, Ernest J. McEachern, Bem Atsma, Siqiao Nan, Yuanxi Zhou, Dominique Schols, Christopher Dennis Smith, Maria Rosaria Di Fluri
  • Patent number: 7053057
    Abstract: This invention provides caspase inhibitors having the formula: wherein Ring A is an optionally substituted piperidine, tetrahydroquinoline or tetrahydroisoquinoline ring; R1 is hydrogen, CHN2, R, or —CH2Y; R is an optionally substituted group selected from an aliphatic group, an aryl group, an aralkyl group, a heterocyclic group, or an heterocyclylalkyl group; Y is an electronegative leaving group; R2 is CO2H, CH2CO2H, or esters, amides or isosteres thereof; Ar is an optionally substituted aryl group; and R3 is hydrogen, an optionally substituted C1-6 alkyl, F2, CN, aryl or R3 is attached to Ar to form an unsaturated or partially saturated five or six membered fused ring having 0–2 heteroatoms. The compounds are useful for treating caspase-mediated diseases in mammals.
    Type: Grant
    Filed: May 23, 2001
    Date of Patent: May 30, 2006
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: Julian M. C. Golec, David Bebbington, Guy Brenchley, Ronald Knegtel, Michael Mortimore
  • Patent number: 7049325
    Abstract: This invention relates to compounds, which are generally anti-inflammatory and analgesic compounds, and which are represented by Formula I: wherein A is a CH2, CH(OH), C(O), C?NOR4, NR5, O, S, S(O), or S(O)2, and the other substituents are as defined in the specification; or prodrugs, individual isomers, mixtures of isomers, and pharmaceutically acceptable salts thereof.
    Type: Grant
    Filed: August 7, 2001
    Date of Patent: May 23, 2006
    Assignee: Syntex (U.S.A.) LLC
    Inventors: Chris Allen Broka, Woongki Kim, David Bernard Smith, Kevin L. McLaren
  • Patent number: 7041829
    Abstract: This invention provides a class of therapeutic compounds and methods for the treatment of mammals with physiological disorders, such as for example a frequently occurring type of essential hypertension, which are critically associated with the decreased binding of magnesium to the plasma membranes of their cells. These methods consist of administering to a mammal in need of such treatment a compound selected from a series of disubstituted trans, trans 1,3-butadienes, 1,3-disubstituted perhydrobutadienes, 1,2-disubstituted trans ethylenes and 1,2 disubstituted ethanes and disubstituted propanes, each of which embodies, in common, the unique structural feature essential for the biological activity of these compounds. This invention also provides for pharmaceutical formulations that employ these novel compounds.
    Type: Grant
    Filed: December 21, 2004
    Date of Patent: May 9, 2006
    Assignee: Magnesium Diagnostics, Inc.
    Inventor: Ibert Clifton Wells
  • Patent number: 6992092
    Abstract: The present invention provides compounds of formula (I) the stereoisomers and prodrugs thereof, and the pharmaceutically acceptable salts of the compounds, stereoisomers, and prodrugs; wherein R1, R2, Ra, Rb, X, and Z are as defined herein; pharmaceutical compositions thereof; and uses thereof.
    Type: Grant
    Filed: April 15, 2004
    Date of Patent: January 31, 2006
    Assignee: Pfizer Inc.
    Inventors: Donald L. Bussolotti, Ronald B. Gammill
  • Patent number: 6951870
    Abstract: Compounds of formula I? wherein the two —OH substituents in the phenyl moiety are in a position ortho to one another and R1 in a position ortho to one of the hydroxy groups; and X, R1 to R6 are as defined in disclosure. The compounds exhibit COMT enzyme inhibiting activity, so are useful as COMT inhibitors.
    Type: Grant
    Filed: June 28, 2001
    Date of Patent: October 4, 2005
    Assignee: Orion Corporation
    Inventors: Jarmo Pystynen, Martti Ovaska, Jukka Vidgren, Timo Lotta, Marjo Yliperttula-Ikonen
  • Patent number: 6916813
    Abstract: Compounds having the formula (I), and pharmaceutically acceptable salts thereof, are useful for modulating mitochondrial F1F0 ATPase activity and treating ischemic conditions including myocardial infarction, congestive heart failure, and cardiac arrhythmias.
    Type: Grant
    Filed: December 10, 2002
    Date of Patent: July 12, 2005
    Assignee: Bristol-Myers Squibb Co.
    Inventors: Karnail S. Atwal, Gary J. Grover, Charles Z. Ding, Philip D. Stein, John Lloyd, Saleem Ahmad, Lawrnce G. Hamann, David Green, Francis N. Ferrara
  • Patent number: 6900319
    Abstract: The invention relates to a compound of the formula I: or a salt thereof with a physiologically tolerated acid, or stereoisomers thereof, wherein R1, R2, A, B, C and D have the meanings described in the specification.
    Type: Grant
    Filed: March 19, 2002
    Date of Patent: May 31, 2005
    Assignee: Abbott GmbH & Co. KG
    Inventors: Hans-Joachim Boehm, Hans Wolfgang Höffken, Wilfried Hornberger, Stefan Koser, Helmut Mack, Thomas Pfeiffer, Werner Seitz, Thomas Zierke
  • Patent number: 6777427
    Abstract: Tetrahydroquinoline compounds of general formula (I) or pharmacologically acceptable salts thereof, which have a specific and strong binding affinity for AR, exhibit AR agonism or antagonism, have therapeutic effects on AR-mediated diseases, particularly by not acting excessively on the prostate as AR agonists, but by showing potent action on skeletal muscle tissue and bone tissue; and pharmaceutical compositions comprising the compounds or the salts as active ingredients:
    Type: Grant
    Filed: March 13, 2003
    Date of Patent: August 17, 2004
    Assignee: Kaken Pharmaceutical Co., Ltd.
    Inventors: Motonori Miyakawa, Seiji Amano, Misa Kamei, Keigo Hanada, Kazuyuki Furuya, Noriko Yamamoto