Tricyclo Ring System Having The Diazole Ring As One The Cyclos Patents (Class 548/302.1)
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Publication number: 20120115855Abstract: Provided herein are compounds, pharmaceutical compositions and combination therapies for inhibition of hepatitis C.Type: ApplicationFiled: December 2, 2009Publication date: May 10, 2012Applicant: PRESIDIO PHARMACEUTICALS, INC.Inventors: Leping Li, Min Zhong
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Publication number: 20120108583Abstract: The present invention relates to tricyclic compounds of formula (I) or pharmaceutically acceptable salt thereof as mPGES-1 inhibitors. These compounds are inhibitors of the microsomal prostaglandin E synthase-1 (mPGES-1) enzyme and are therefore useful in the treatment of pain and/or inflammation from a variety of diseases or conditions, such as asthma, osteoarthritis, rheumatoid arthritis, acute or chronic pain and neurodegenerative diseases.Type: ApplicationFiled: October 28, 2011Publication date: May 3, 2012Applicant: Glenmark Pharmaceuticals S.A.Inventors: Laxmikant A. Gharat, Nagarajan Muthukaman, Lakshminarayana Narayana, Neelima Khairatkar-Joshi, Vidya G. Kattige
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Patent number: 8168800Abstract: In one aspect, the present invention provides for compounds and labeled compounds of Formula I, and pharmaceutical compositions thereof. In another aspect, the present invention provides for methods of using compounds or labeled compounds of Formula I for various therapeutic and imaging purposes, including, but not limited to, treating Alzheimer's disease in patient and imaging A? peptide aggregates in a patient.Type: GrantFiled: October 31, 2008Date of Patent: May 1, 2012Assignee: The Regents of the University of CaliforniaInventors: Lee-Way Jin, Kit S. Lam, Ruiwu Liu, Hyun-Seok Hong, Izumi Maezawa
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Publication number: 20120101243Abstract: The present invention provides an article of manufacture formed from a substrate and a benzazoloporphyrazine bound to the substrate. The article may take a variety of different forms and may be for example an electrochromic display, a molecular capacitor, a battery, a solar cell, or a molecular memory device. Methods of making such articles, along with compounds, methods and intermediates useful for making such benzazoloporphyrazines, are also described.Type: ApplicationFiled: December 19, 2011Publication date: April 26, 2012Inventors: W. Justin Youngblood, Jonathan S. Lindsey
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Patent number: 8147818Abstract: The present disclosure relates to compounds, compositions and methods for the treatment of hepatitis C virus (HCV) infection. Also disclosed are pharmaceutical compositions containing such compounds and methods for using these compounds in the treatment of HCV infection.Type: GrantFiled: January 23, 2009Date of Patent: April 3, 2012Assignee: Bristol-Myers Squibb CompanyInventors: Carol Bachand, Makonen Belema, Daniel H. Deon, Andrew C. Good, Jason Goodrich, Clint A. James, Rico Lavoie, Omar D. Lopez, Alain Martel, Nicholas A. Meanwell, Van N. Nguyen, Jeffrey Lee Romine, Edward H. Ruediger, Lawrence B. Snyder, Denis R. St. Laurent, Fukang Yang, David R. Langley, Gan Wang, Lawrence G. Hamann
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Patent number: 8148363Abstract: The present invention relates to novel heterocyclic compounds of Formulae I-III; as disclosed herein or a pharmaceutically acceptable salt, solvate, ester, prodrug or stereoisomer thereof. Also disclosed are pharmaceutical compositions comprising said compounds, and methods for using said compounds for treating or preventing a thromboembolic disorder.Type: GrantFiled: May 18, 2009Date of Patent: April 3, 2012Assignee: Schering CorporationInventors: Martin C. Clasby, William J. Greenlee, Yan Xia, Tin-Yau Chan, Mariappan V. Chelliah, Samuel Chackalamannil, Haiyan Pu, Keith A. Eagen, Henry Vaccaro, Brian A. McKittrick, Liyuan Wang, Xiaobang Gao
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Publication number: 20120040977Abstract: Provided herein are compounds, pharmaceutical compositions and combination therapies for inhibition of hepatitis C.Type: ApplicationFiled: February 22, 2010Publication date: February 16, 2012Applicant: PRESIDIO PHARMACEUTICALS, INC.Inventors: Leping Li, Min Zhong
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Patent number: 8110575Abstract: The present invention relates to new CGRP-antagonists of general formula I wherein U, V, X, Y, R1, R2, R3 and R4 are defined as in the description, the tautomers, the isomers, the diastereomers, the enantiomers, the hydrates, the mixtures thereof and the salts thereof and the hydrates of the salts, particularly the physiologically acceptable salts thereof with inorganic or organic acids or bases, medicaments containing these compounds, their use and processes for preparing them.Type: GrantFiled: November 21, 2008Date of Patent: February 7, 2012Assignee: Boehringer Ingelheim International GmbHInventors: Dirk Gottschling, Georg Dahmann, Henri Doods, Annekatrin Heimann, Stephan Georg Mueller, Klaus Rudolf, Gerhard Georg Schaenzle, Dirk Stenkamp
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Publication number: 20120004384Abstract: The present invention provides an article of manufacture formed from a substrate and a benzazoloporphyrazine bound to the substrate. The article may take a variety of different forms and may be for example an electrochromic display, a molecular capacitor, a battery, a solar cell, or a molecular memory device. Methods of making such articles, along with compounds, methods and intermediates useful for making such benzazoloporphyrazines, are also described.Type: ApplicationFiled: February 25, 2011Publication date: January 5, 2012Inventors: W. Justin Youngblood, Jonathan S. Lindsey
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Patent number: 8076365Abstract: The present invention relates to compounds represented by formula (I) wherein A, B, D, E, R2, R3, R4, R5, R6, R9, a, b, d and e are as defined herein, their salt or ester and pharmaceutical compositions thereof useful in the treatment of hepatitis C viral (HCV) infection. Said compounds were found to have inhibitory activity against HCV polymerase, especially as inhibitors of HCV NS5B polymerase.Type: GrantFiled: August 3, 2006Date of Patent: December 13, 2011Assignee: Boehringer Ingelheim International GmbHInventor: Youla S. Tsantrizos
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Patent number: 8039532Abstract: A compound represented by formula (I-1): wherein R21, R22, R23 and R24 each independently represent a hydrogen atom or a monovalent substituent, with the proviso that compounds, in which R21, R22, R23 and R24 each are an alkylthio group, are excluded; R21 and R22 and/or R23 and R24 each may bond to each other to form a ring, with the proviso that compounds, in which the formed ring is a dithiol ring or a dithiolane ring, are excluded; R25 and R26 each independently represent a hydrogen atom or a monovalent substituent; X21, X22, X23 and X24 each independently represent a hetero atom; compounds, wherein R21, R22, R23 and R24 each represent a cyan group; X21, X22, X23 and X24 each represent a sulfur atom; and R25 and R26 each represent a hydroxyl group or a hydrogen atom, are excluded; and compounds, wherein R21 and R23 each represent a hydrogen atom; R22 and R24 each represent an arylcarbonyl group; X21, X22, X23 and X24 each represent a sulfur atom; and R25 and R26 each represent a hydroxyl group, are eType: GrantFiled: August 15, 2008Date of Patent: October 18, 2011Assignee: Fujifilm CorporationInventors: Naoyuki Hanaki, Masuji Motoki, Toshihiko Yawata
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Patent number: 8039484Abstract: Diaryl ethers in which one of the aryl groups is a phenyl fused to a cycloalkyl or heterocyclic ring, to which is attached an acetic acid group, are agonists of G-protein coupled receptor 40 (GPR40) and are useful as therapeutic compounds, particularly in the treatment of Type 2 diabetes mellitus, and of conditions that often accompany this disease, including insulin resistance, obesity and lipid disorders.Type: GrantFiled: October 26, 2007Date of Patent: October 18, 2011Assignee: Merck Sharp & Dohme Corp.Inventors: Min Ge, Songnian Lin, Shawn P. Walsh, Lihu Yang, Changyou Zhou
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Publication number: 20110195044Abstract: The present disclosure relates to compounds, compositions and methods for the treatment of hepatitis C virus (HCV) infection. Also disclosed are pharmaceutical compositions containing such compounds and methods for using these compounds in the treatment of HCV infection.Type: ApplicationFiled: July 29, 2010Publication date: August 11, 2011Inventor: Jeffrey Lee Romine
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Patent number: 7964598Abstract: The present invention provides compounds that inhibit apoE4 domain interaction; and compositions, including pharmaceutical compositions, comprising the compounds. The present invention provides methods of treating apoE4-related disorders. The methods generally involve administering to an individual in need thereof a therapeutically effective amount of an apoE4 domain interaction inhibitor.Type: GrantFiled: October 4, 2005Date of Patent: June 21, 2011Assignee: The J. David Gladstone InstitutesInventors: Robert W. Mahley, Karl H. Weisgraber, Yadong Huang
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Patent number: 7939555Abstract: Pharmaceutical formulations and methods including an immune response modifier (IRM) compound and an oleic acid component are provided where stability is improved by using oleic acid have low polar impurities such as peroxides.Type: GrantFiled: February 1, 2010Date of Patent: May 10, 2011Assignee: 3M Innovative Properties CompanyInventors: Alexis S. Statham, Robert J. Nelson
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Publication number: 20110098327Abstract: This disclosure concerns novel compounds of Formula (I) or Formula (II) as defined in the specification and compositions comprising such novel compounds. These compounds are useful antiviral agents, especially in inhibiting the function of the NS5A protein encoded by Hepatitis C virus (HCV). Thus, the disclosure also concerns a method of treating HCV related diseases or conditions by use of these novel compounds or a composition comprising such novel compounds.Type: ApplicationFiled: April 7, 2010Publication date: April 28, 2011Inventors: Rico Lavoie, John A. Bender, Carol Bachand, Edward H. Ruediger, John F. Kadow
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Patent number: 7928119Abstract: Methods of treating IL-6 involved diseases with EP4 receptor ligands, including EP4 receptor antagonists. Assays to determine the effect of test compounds on PGE2-induced whole blood cells activation.Type: GrantFiled: November 3, 2006Date of Patent: April 19, 2011Assignee: Pfizer Inc.Inventors: Masato Shimojo, Kana Taniguchi
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Patent number: 7923463Abstract: Pharmaceutical formulations and methods including an immune response modifier (IRM) compound and an oleic acid component are provided where stability is improved by using oleic acid have low polar impurities such as peroxides.Type: GrantFiled: February 1, 2010Date of Patent: April 12, 2011Assignee: 3M Innovative Properties CompanyInventors: Alexis S. Statham, Robert J. Nelson
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Publication number: 20110077280Abstract: This disclosure concerns novel compounds of Formula (I) as defined in the specification and compositions comprising such novel compounds. These compounds are useful antiviral agents, especially in inhibiting the function of the NS5A protein encoded by Hepatitis C virus (HCV). Thus, the disclosure also concerns a method of treating HCV related diseases or conditions by use of these novel compounds or a composition comprising such novel compounds.Type: ApplicationFiled: March 23, 2010Publication date: March 31, 2011Inventors: John A. Bender, Piyasena Hewawasam, John F. Kadow, Omar D. Lopez, Nicholas A. Meanwell, Van N. Nguyen, Jeffrey Lee Romine, Lawrence B. Snyder, Denis R. St. Laurent, Gan Wang, Ningning Xu, Makonen Belema
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Publication number: 20110071301Abstract: In one aspect, the present invention provides for compounds and labeled compounds of Formula I, and pharmaceutical compositions thereof. In another aspect, the present invention provides for methods of using compounds or labeled compounds of Formula I for various therapeutic and imaging purposes, including, but not limited to, treating Alzheimer's disease in patient and imaging A? peptide aggregates in a patient.Type: ApplicationFiled: October 31, 2008Publication date: March 24, 2011Applicant: The Regents of the University of CaliforniaInventors: Lee-way Jin, Kit S. Lam, Ruiwu Liu, Hyun-Seok Hong, Izumi Maezawa
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Publication number: 20110065682Abstract: The present invention relates to novel heterocyclic compounds of Formulae I-III; as disclosed herein or a pharmaceutically acceptable salt, solvate, ester, prodrug or stereoisomer thereof. Also disclosed are pharmaceutical compositions comprising said compounds, and methods for using said compounds for treating or preventing a thromboembolic disorder.Type: ApplicationFiled: May 18, 2009Publication date: March 17, 2011Inventors: Martin C. Clasby, William J. Greenlee, Yan Xia, Tin-Yau Chan, Mariappan V. Chelliah, Samuel Chackalamannil, Haiyan Pu,, Keith A. Eagen, Henry Vaccaro, Brian A. McKittrick,, Liyuan Wang, Xiaobang Gao
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Patent number: 7906543Abstract: Pharmaceutical formulations and methods including an immune response modifier (IRM) compound and an oleic acid component are provided where stability is improved by using oleic acid have low polar impurities such as peroxides.Type: GrantFiled: January 29, 2010Date of Patent: March 15, 2011Assignee: 3M Innovative Properties CompanyInventors: Alexis S. Statham, Robert J. Nelson
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Patent number: 7902243Abstract: Pharmaceutical formulations and methods including an immune response modifier (IRM) compound and an oleic acid component are provided where stability is improved by using oleic acid have low polar impurities such as peroxides.Type: GrantFiled: February 1, 2010Date of Patent: March 8, 2011Assignee: 3M Innovative Properties CompanyInventors: Alexis S. Statham, Robert J. Nelson
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Patent number: 7902244Abstract: Pharmaceutical formulations and methods including an immune response modifier (IRM) compound and an oleic acid component are provided where stability is improved by using oleic acid have low polar impurities such as peroxides.Type: GrantFiled: February 1, 2010Date of Patent: March 8, 2011Assignee: 3M Innovative Properties CompanyInventors: Alexis S. Statham, Robert J. Nelson
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Patent number: 7902242Abstract: Pharmaceutical formulations and methods including an immune response modifier (IRM) compound and an oleic acid component are provided where stability is improved by using oleic acid have low polar impurities such as peroxides.Type: GrantFiled: January 30, 2010Date of Patent: March 8, 2011Assignee: 3M Innovative Properties CompanyInventors: Alexis S. Statham, Robert J. Nelson
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Patent number: 7902246Abstract: Pharmaceutical formulations and methods including an immune response modifier (IRM) compound and an oleic acid component are provided where stability is improved by using oleic acid have low polar impurities such as peroxides.Type: GrantFiled: February 1, 2010Date of Patent: March 8, 2011Assignee: 3M Innovative Properties CompanyInventors: Alexis S. Statham, Robert J. Nelson
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Publication number: 20110046132Abstract: The present invention is directed to benzoimidazole compounds of the formula (1) and enantiomers, diastereomers, racemates, and pharmaceutically acceptable salts thereof. Compounds of the present invention are useful in pharmaceutical compositions and methods for the treatment of disease states, disorders, and conditions modulated by prolyl hydroxylase activity.Type: ApplicationFiled: April 28, 2009Publication date: February 24, 2011Inventors: Frances Meredith Hocutt, Barry Eastman Leonard, JR., Hillary M. Peltier, Victor K. Phuong, Michael H. Rabinowitz, Mark D. Rosen, Kyle T. Tarantino, Hariharan Venkatesan, Lucy Xiumin Zhao
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Patent number: 7863310Abstract: The present invention provides kinase inhibitors of Formula I:Type: GrantFiled: January 21, 2005Date of Patent: January 4, 2011Assignee: Eli Lilly and CompanyInventors: Rosanne Bonjouklian, Robert Dean Dally, Alfonso de Dios, Mirian Filadelfa del Prado Catalina, Carmen Dominguez-Fernandez, Carlos Jaramillo Aguado, Beatriz Lopez de Uralde-Garmendia, Timothy Alan Shepherd
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Publication number: 20100298287Abstract: There is provided a compound of the formula (I?): wherein X is a nitrogen or CRx, Rx is a hydrogen, etc., R1 is an optionally substituted hydrocarbon group, etc., R2 is an optionally substituted hydrocarbon group, etc., ring A is 5- to -8-membered heterocyclic ring, etc., and each of Y1, Y2 and Y3 is an optionally substituted carbon or a nitrogen, etc.; or ‘a salt thereof or a prodrug thereof, which have CRF receptor antagonistic activity and use thereof.Type: ApplicationFiled: January 21, 2009Publication date: November 25, 2010Inventors: Kazuyoshi Aso, Katsumi Kobayashi, Takafumi Takai, Takuto Kojima, Kazuyuki Tokumaru, Michiyo Mochizuki, Yasutaka Hoashi
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Publication number: 20100249085Abstract: This invention relates to novel heteroaryl substituted pyrazole compounds, pharmaceutical compositions containing such compounds and the use of those compounds or compositions for treating hyper-proliferative and/or angiogenesis disorders, as a sole agent or in combination with other active ingredients or therapeutic measures.Type: ApplicationFiled: May 8, 2008Publication date: September 30, 2010Applicant: BAYER SCHERING PHARMA AKTIENGESELLSCHAFTInventors: Stephen Boyer, Michael Härter, Philip L. Wickens, Manoj Patel, Ellalahewage Sathyajith Kumarasinghe, Ajay Kumar Bhargava, Karl-Heinz Thierauch, Hartmut Beck, Susanne Greschat, Peter Ellinghaus, Patrick Paulus, Holger Hess-Stumpp
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Publication number: 20100244006Abstract: An organic electroluminescent device is provided and includes: a cathode; an anode; and at least one organic layer between the cathode and the anode. The at least one organic layer includes a light emitting layer containing at least one light emitting material. A compound represented by the following formula (I) is contained in the at least one organic layer. where n stands for an integer of 2 or greater, L represents an n-valent linking group, and R1, R2, R3, and R4 each independently represents a hydrogen atom or a substituent.Type: ApplicationFiled: March 25, 2010Publication date: September 30, 2010Applicant: FUJIFILM CORPORATIONInventors: Toshihiro ISE, Wataru SOTOYAMA
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Publication number: 20100215616Abstract: The present disclosure relates to compounds, compositions and methods for the treatment of hepatitis C virus (HCV) infection. Also disclosed are pharmaceutical compositions containing such compounds and methods for using these compounds in the treatment of HCV infection.Type: ApplicationFiled: February 8, 2010Publication date: August 26, 2010Inventors: Jeffrey Lee Romine, Denis R. St. Laurent, Makonen Belema, Lawrence B. Snyder, Lawrence G. Hamann, John F. Kadow, Jayne Kapur, Andrew C. Good, Omar D. Lopez, Rico Lavoie, John A. Bender
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Publication number: 20100216988Abstract: The present invention relates to a process for the regioselective synthesis of compounds of the formula I, wherein R1; R2; R3; R4; J1; J2; J3; J4 and G have the meanings indicated in the claims. The present invention provides a direct metal, e.g. palladium or copper, catalyzed, regioselective process to a wide variety of unsymmetrical, multifunctional N-substituted benzimidazoles or azabenzimidazoles of formula I starting from 2-halo-nitroarenes and N-substituted amides.Type: ApplicationFiled: December 22, 2009Publication date: August 26, 2010Applicant: SANOFI-AVENTISInventors: Jorge ALONSO, Andreas LINDENSCHMIDT, Marc NAZARE, Omar RKYEK, Matthias URMANN, Nis HALLAND
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Publication number: 20100210762Abstract: A compound represented by formula (I-1): wherein R21, R22, R23 and R24 each independently represent a hydrogen atom or a monovalent substituent, with the proviso that compounds, in which R21, R22, R23 and R24 each are an alkylthio group, are excluded; R21 and R22 and/or R23 and R24 each may bond to each other to form a ring, with the proviso that compounds, in which the formed ring is a dithiol ring or a dithiolane ring, are excluded; R25 and R26 each independently represent a hydrogen atom or a monovalent substituent; X21, X22, X23 and X24 each independently represent a hetero atom; compounds, wherein R21, R22, R23 and R24 each represent a cyan group; X21, X22, X23 and X24 each represent a sulfur atom; and R25 and R26 each represent a hydroxyl group or a hydrogen atom, are excluded; and compounds, wherein R21 and R23 each represent a hydrogen atom; R22 and R24 each represent an arylcarbonyl group; X21, X22, X23 and X24 each represent a sulfur atom; and R25 and R26 each represent a hydroxyl group, are eType: ApplicationFiled: August 15, 2008Publication date: August 19, 2010Applicant: FUJIFILM CORPORATIONInventors: Naoyuki Hanaki, Masuji Motoki, Toshihiko Yawata
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Publication number: 20100173897Abstract: The present invention discloses and claims a series of substituted N-phenyl-bipyrrolidine carboxamides of formula (I). Wherein R, R1, R2, R3 and R4 are as described herein. More specifically, the compounds of this invention are modulators of H3 receptors and are, therefore, useful as pharmaceutical agents, especially in the treatment and/or prevention of a variety of diseases modulated by H3 receptors including diseases associated with the central nervous system. Additionally, this invention also discloses methods of preparation of substituted N-phenyl-bipyrrolidine carboxamides and intermediates therefor.Type: ApplicationFiled: March 15, 2010Publication date: July 8, 2010Applicant: SANOFI-AVENTISInventors: Werngard CZECHTIZKY, Zhongli GAO, William J. HURST, Lothar SCHWINK, Siegfried STENGELIN
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Publication number: 20100168098Abstract: The present invention relates to compounds represented by formula (I) wherein A, B, D, E, R2, R3, R4, R5, R6, R9, a, b, d and e are as defined herein, their salt or ester and pharmaceutical compositions thereof useful in the treatment of hepatitis C viral (HCV) infection.Type: ApplicationFiled: August 3, 2006Publication date: July 1, 2010Inventor: Youla S. Tsantrizos
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Patent number: 7741355Abstract: Provided are small-molecule Trp-p8 modulators, including Trp-p8 agonists and Trp-p8 antagonists, and compositions comprising small-molecule Trp-p8 agonists as well as methods for identifying and characterizing novel small-molecule Trp-p8 modulators and methods for decreasing viability and/or inhibiting growth of Trp-p8 expressing cells, methods for activating Trp-p8-mediated cation influx, methods for stimulating apoptosis and/or necrosis, and related methods for the treatment of diseases, including cancers such as lung, breast, colon, and/or prostate cancers as well as other diseases, such as benign prostatic hyperplasia, that are associated with Trp-p8 expression.Type: GrantFiled: February 15, 2007Date of Patent: June 22, 2010Assignee: Dendreon CorporationInventors: Ofir Moreno, Sateesh Natarajan, David F. Duncan
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Patent number: 7732435Abstract: The invention relates to novel heterocyclic compounds of the formula in which all of the variables are as defined in the specification, in free form or in salt form, to their preparation, to their use as medicaments and to medicaments comprising them.Type: GrantFiled: December 5, 2006Date of Patent: June 8, 2010Assignee: Novartis AGInventors: Andrew James Culshaw, Christopher Thomas Brain, Edward Karol Dziadulewicz, Lee Edwards, Terance William Hart, Timothy John Ritchie
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Publication number: 20100130513Abstract: Provided are compounds of the formula: wherein RN1 is a substituent of formula G1-NX1X2, wherein G1 is an optionally further substituted alkylene, which optionally forms, together with RN2, a cyclic group, and each of X1 and X2 is independently H or an N-substituent, or X1 and X2 together form a heterocyclic ring, or X1 together with G1 forms a cyclic group and X2 is H or an N-substituent; and each of Z1, Z2, Z3 and Z4 is H or a substituent, or two of Z1, Z2, Z3 and Z4 together form an optionally substituted ring, and further wherein at least one of Z1, Z2, Z3 and Z4 is other than H, and salts thereof, pharmaceutical compositions and methods of using the compounds. The compounds have antiviral activity.Type: ApplicationFiled: November 17, 2009Publication date: May 27, 2010Applicant: Isis Pharmaceuticals, Inc.Inventors: Punit P. Seth, Elizabeth Anne Jefferson, Richard H. Griffey, Eric E. Swayze
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Patent number: 7714010Abstract: The invention relates to pyrrolobenzimidazolone compounds of formula (I), wherein A, T and R1 to R3 are defined as in claim 1, which are suitable for the treatment of diseases characterized by excessive or abnormal cell proliferation and the use thereof for preparing a pharmaceutical composition.Type: GrantFiled: May 17, 2005Date of Patent: May 11, 2010Assignee: Boehringer Ingelheim International GmbHInventors: Darryl McConnel, Steffen Steurer, Bernd Krist, Ulrike Weyer-Czernilofsky, Maria Impagnatiello, Matthias Treu, Iris Kauffmann-Hefner, Pilar Garin-Chesa, Andreas Schnapp
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Patent number: 7713975Abstract: Methods for treating an allergic or inflammatory disease or other Syk-mediated disease or Syk-mediated condition characterized by administering a composition which contains a therapeutically effective amount of a 3,6-substituted imidazol[1,2-b]pyridazine compound.Type: GrantFiled: January 12, 2006Date of Patent: May 11, 2010Assignee: Alcon, Inc.Inventors: Mark R. Hellberg, Steven T. Miller, Andrew Rusinko
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Publication number: 20100113423Abstract: The present disclosure provides compounds that function as modulators of aldehyde dehydrogenase (ALDH) enzymatic activity, as well as compositions and formulations comprising the compounds. The present disclosure provides therapeutic methods involving administering a subject compound, or a subject pharmaceutical composition.Type: ApplicationFiled: October 19, 2009Publication date: May 6, 2010Inventors: Daria Mochly-Rosen, Che-Hong Chen, Wenjin Yang
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Publication number: 20100105725Abstract: Diaryl ethers in which one of the aryl groups is a phenyl fused to a cycloalkyl or heterocyclic ring, to which is attached an acetic acid group, are agonists of G-protein coupled receptor 40 (GPR40) and are useful as therapeutic compounds, particularly in the treatment of Type 2 diabetes mellitus, and of conditions that often accompany this disease, including insulin resistance, obesity and lipid disorders.Type: ApplicationFiled: October 26, 2007Publication date: April 29, 2010Inventors: Min Ge, Songnian Lin, Shawn P. Walsh, Lihu Yang, Changyou Zhou
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Publication number: 20100098634Abstract: Provided herein are compounds and compositions which comprise the formulae as disclosed herein, wherein the compound is an amyloid binding compound. An amyloid binding compound according to the invention may be administered to a patient in amounts suitable for in vivo imaging of amyloid deposits, and distinguish between neurological tissue with amyloid deposits and normal neurological tissue. Amyloid probes of the invention may be used to detect and quantitate amyloid deposits in diseases including, for example, Down's syndrome, familial Alzheimer's Disease. In another embodiment, the compounds may be used in the treatment or prophylaxis of neurodegenerative disorders. Also provided herein are methods of allowing the compound to distribute into the brain tissue, and imaging the brain tissue, wherein an increase in binding of the compound to the brain tissue compared to a normal control level of binding indicates that the mammal is suffering from or is at risk of developing a neurodegenerative disease.Type: ApplicationFiled: July 24, 2009Publication date: April 22, 2010Inventors: Hartmuth C. Kolb, Joseph C. Walsh, Wei Zhang, Umesh B. Gangadharmath, Dhanalakshmi Kasi, Kai Chen, Anjana Sinha, Eric Wang, Gang Chen, Peter J.H. Scott, Henry Clifton Padgett, Qianwa Liang, Zhiyong Gao, Tieming Zhao, Chunfang Xia
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Publication number: 20100069374Abstract: This invention relates to benzopyran derivatives of formula (I) or (II), or pharmaceutically acceptable salts thereof wherein R1 and R2 are independently of each other hydrogen atom, C1-6alkyl group or C6-14aryl group, R3 is hydrogen atom or C1-6alkylcarbonyloxy group, or together with R4 forms a bond, R4 is hydrogen atom, or together with R3 forms a bond, m is an integer of 0 to 4, n is an integer of 0 to 4, V is a single bond, CR7R8, NR9, O, S, SO or SO2, R5 is hydrogen atom or C1-6alkyl group, R6 is hydrogen atom, C1-6alkyl group, C3-8cycloalkyl group, C3-8cycloalkenyl group, amino group, C1-6alkylamino group, di-C1-6alkylamino group, C6-14arylamino group, C2-9heteroarylamino group, C6-14aryl group, C2-9heteroaryl group or C2-9heterocyclyl group, A is 5-, 6- or 7-member ring fused with benzene ring, as constituent atom of the ring, oxygen atom, nitrogen atom or sulfur atom may be contained in the number of 1 to 3 alone or in a combination thereof, the number of unsaturated bond in the ring is 1, 2 or 3Type: ApplicationFiled: November 17, 2009Publication date: March 18, 2010Applicant: NISSAN CHEMICAL INDUSTRIES, LTD.Inventors: Kazuhiko Ohrai, Yukohiro Shigeta, Osamu Uesugi, Takumi Okada, Tomoyuki Matsuda
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Publication number: 20100048532Abstract: This invention relates to compounds of the formula (I): or a pharmaceutically acceptable salt thereof, wherein: R1, R2, R3, R4, A and E are each as described herein or a pharmaceutically acceptable salt, and compositions containing such compounds and the method of treatment and the use, comprising such compounds for the treatment of a condition mediated by acid pump antagonistic activity such as, but not limited to, as gastrointestinal disease, gastroesophageal disease, gastroesophageal reflux disease (GERD), laryngopharyngeal reflux disease, peptic ulcer, gastric ulcer, duodenal ulcer, NSAID-induced ulcers, gastritis, infection of Helicobacter pylori, dyspepsia, functional dyspepsia, Zolli?ger-Ellison syndrome, non-erosive reflux disease (NERD), visceral pain, cancer, heartburn, nausea, esophagitis, dysphagia, hypersalivation, airway disorders or asthma.Type: ApplicationFiled: September 17, 2007Publication date: February 25, 2010Applicant: RaQualia Pharma Inc.Inventors: Hiroki Koike, Mikio Morita
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Publication number: 20100022547Abstract: One aspect of the present invention relates to compounds, and pharmaceutically acceptable salts and prodrugs thereof, that are useful as inhibitors of IMPDH. The invention also provides pharmaceutical compositions comprising the compounds of the invention which selectively inhibit parasitic IMPDH. In certain embodiments, the present invention relates to selective inhibition of C. parvum inosine-5?-monophosphate-dehydrogenase over human inosine-5?-monophosphate-dehydrogenase (IMPDH type I and type II). These compounds may be used alone or in combination with other therapeutic or prophylactic agents, such as anti-virals, anti-inflammatory agents, antimicrobials and immunosuppressants.Type: ApplicationFiled: June 1, 2007Publication date: January 28, 2010Applicants: BRANDEIS UNIVERSITY, UNIVERSITY OF GEORFIA RESEARCH FOUNDATIONInventors: Lizbeth K. Hedstrom, Boris Striepen
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Publication number: 20100010038Abstract: The present invention provides a compound represented by the formula wherein R1 is a hydrocarbon group optionally having substituent(s), amino optionally having substituent(s), hydroxy optionally having a substituent or a heterocyclic group optionally having substituent(s), R2 is a hydrogen atom or a hydrocarbon group optionally having substituent(s), R3 is a hydrogen atom, a halogen atom, a hydrocarbon group optionally having substituent(s), amino optionally having substituent(s), hydroxy optionally having a substituent or mercapto optionally having a substituent, Xa, Xb, Xc and Xd are each a carbon atom or a nitrogen atom, provided that any one or two of Xa, Xb, Xc and Xd is/are nitrogen atom(s), m is 0 to 2, and rings A to C are each a ring optionally having substituent(s), or a salt thereof, which is useful as an agent for the prophylaxis or treatment of a disease relating to an action of melatonin, and the like.Type: ApplicationFiled: December 27, 2007Publication date: January 14, 2010Inventors: Osamu Uchikawa, Tatsuki Koike, Takafumi Takai, Yasutaka Hoashi
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Publication number: 20090318445Abstract: The invention relates to novel compounds that are inhibitors of peptidyl deformylase (PDF). The compounds are useful as antimicrobials and antibiotics. The compounds of the invention display selective inhibition of peptidyl deformylase versus other metalloproteinases such as MMPs. Methods of preparation and uses of the compounds are also disclosed.Type: ApplicationFiled: December 28, 2006Publication date: December 24, 2009Applicants: NORVARTIS AG, NOVARTIS PHARMA GMBHInventors: Arkadius Pichota, Jeyaraj Duraiswamy, Zheng Yin, Thomas Hugo Keller, Mark Schreiber
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Patent number: 7632578Abstract: An emitting compound for an organic electroluminescent device, and an organic electroluminescent device using the same, supply an effective luminance, an efficient driving voltage, and color purity. The emitting compound has an imidazo-pyridine frame represented as in the following Formula 1: where R1 to R14, each of which is independent, refer to the functional groups recited herein.Type: GrantFiled: February 4, 2004Date of Patent: December 15, 2009Assignee: Samsung Mobile Display Co., Ltd.Inventors: Seok-Jong Lee, Yong-Joong Choi