Nitrogen Attached Indirectly To The Diazole Ring By Acyclic Nonionic Bonding Patents (Class 548/309.7)
  • Publication number: 20130059852
    Abstract: Some embodiments of this invention include methods for treating disease and methods for administering a compound of Formula (I). In some aspects of the invention, diseases can be treated by administration of compositions comprising a compound of Formula (I). Pharmaceutical compositions of some embodiments of the present invention comprise a compound of Formula (I).
    Type: Application
    Filed: April 8, 2011
    Publication date: March 7, 2013
    Applicant: UNIVERSITY OF LOUISVILLE RESEARCH FOUNDATION, INC.
    Inventors: John O. Trent, Jason B. Meier, Kelby B. Napier
  • Publication number: 20130029846
    Abstract: The present invention relates to the use of bicyclic amidine compounds of formula I as defined in the description, and the N-oxides, and salts thereof for combating harmful fungi, and also to compositions and seed comprising at least one such compound. The invention also relates to novel bicyclic amidines and processes and intermediates for preparing these compounds.
    Type: Application
    Filed: March 28, 2011
    Publication date: January 31, 2013
    Applicant: BASF SE
    Inventors: Joachim Rheinheimer, Christian Pilger, Stefan Redlich, Doris Kremzow, Claudia Rosenbaum, Burghard Liebmann, Wassilios Grammenos
  • Publication number: 20130029964
    Abstract: An object of the present invention is to provide a novel low molecular weight compound exhibiting an osteogenesis-promoting action. This object is achieved by a compound having the general formula (I) or a pharmacologically acceptable salt thereof. In the general formula (I), R1 and R2 represent hydrogen atoms, and the like; R3 represents a hydrogen atom, and the like; X, Y, and Z represent nitrogen atoms, and the like; A represents a phenylene group, and the like; n represents 1 or 2, and the like; and V and W represent oxygen atoms, and the like.
    Type: Application
    Filed: August 27, 2012
    Publication date: January 31, 2013
    Applicant: DAIICHI SANKYO COMPANY, LIMITED
    Inventors: Kazumasa Aoki, Satoshi Matsui, Kenji Yoshikawa, Hiroki Shimizu, Junko Sasaki, Katsuyoshi Nakajima, Osamu Kanno, Kiyoshi Oizumi
  • Patent number: 8354543
    Abstract: The invention relates to a process for preparing an optionally substituted 4-benzimidazol-2-ylmethylamino)-benzamidine, characterized in that (a) an optionally correspondingly substituted diaminobenzene is condensed with 2-[4-(1,2,4-oxadiazol-5-on-3-yl)-phenylamino]-acetic acid, (b) i) the product thus obtained is hydrogenated and ii) optionally the amidino group is carbonylated, without isolating the intermediate product of the hydrogenation beforehand; as well as a process for preparing a salt of an optionally substituted 4-(benzimidazol-2-ylmethylamino)-benzamidine, wherein (a) an optionally correspondingly substituted diaminobenzene is condensed with 2-[4-(1,2,4-oxadiazol-5-on-3-yl)-phenylamino]-acetic acid, (b) the product thus obtained is hydrogenated, and (c) i) optionally the amidino group is carbonylated and ii) without prior isolation of the intermediate product of the carbonylation the desired salt is isolated.
    Type: Grant
    Filed: April 29, 2010
    Date of Patent: January 15, 2013
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Georg Zerban, Arndt Hausherr, Kerstin Schlarb, Rainer Hamm, Gunter Koch, Bjoem Weyell, Heinz-Peter Schmitt
  • Publication number: 20120330025
    Abstract: A novel triarylamine compound having a bipolar property is provided. The triarylamine compound can be used for a hole-injection layer, a hole-transport layer, a light-emitting layer, or an electron-transport layer in a light-emitting element. The triarylamine compound can also be used as a host material with a light-emitting material which emits relatively short-wavelength light, in a structure where the host material and the guest material constitute a light-emitting layer. The triarylamine compound of the present invention is a fluorescent compound and therefore can also be used as a light-emitting substance of a light-emitting layer. A light-emitting element having high emission efficiency is provided. A light-emitting device, an electronic device, or a lighting device having low power consumption is provided.
    Type: Application
    Filed: June 21, 2012
    Publication date: December 27, 2012
    Inventors: Harue Osaka, Takahiro Ushikubo, Tsunenori Suzuki, Nobuharu Ohsawa
  • Publication number: 20120316201
    Abstract: The invention relates to novel benzimidazole and imidazopyridine derivatives having the general Formula (I), which have a good affinity with certain subtypes of melanocortin receptors, particularly MC4 receptors. The derivatives are particularly suitable for the treatment of pathological states and diseases involving one or more melanocortin receptors. The invention also relates to pharmaceutical compositions containing said the compounds having the general Formula (I).
    Type: Application
    Filed: June 8, 2012
    Publication date: December 13, 2012
    Applicant: IPSEN PHARMA S.A.S.
    Inventors: Lÿdie POITOUT, Valerie Brault, Carole Sackur, Pierre Roubert, Pascale Plas
  • Patent number: 8314253
    Abstract: The invention relates to compounds of formula (I) wherein R1, R2, R3, R4, A, B, W and n are as defined in the description, and to pharmaceutically acceptable salts of such compounds. These compounds are useful as calcium channel blockers.
    Type: Grant
    Filed: October 21, 2009
    Date of Patent: November 20, 2012
    Assignee: Actelion Pharmaceuticals Ltd.
    Inventors: Kurt Hilpert, Francis Hubler, Dorte Renneberg
  • Publication number: 20120184518
    Abstract: Methods for the treatment and/or prevention of an inflammatory disease or disorder through administration of an inhibitor of a glutaminyl peptide cyclotransferase. Inflammatory diseases or disorders treated or prevented by methods disclosed herein include mild cognitive impairment (MCI), rheumatoid arthritis, atherosclerosis, restenosis, pancreatitis, sepsis and peritonitus. Further provided are respective diagnostic methods, assays and kits.
    Type: Application
    Filed: January 20, 2012
    Publication date: July 19, 2012
    Applicant: PROBIODRUG AG
    Inventors: Stephan Schilling, Holger Cynis, Torsten Hoffman, Hans-Ulrich Demuth
  • Patent number: 8217070
    Abstract: Compounds of Formula (I) inhibit the PARP enzyme and are useful for treating a disease or a disorder associated with PARP. Also disclosed are pharmaceutical compositions comprising compounds of Formula (I), methods of treatment comprising compounds of Formula (I), and methods of inhibiting the PARP enzyme comprising compounds of Formula (I).
    Type: Grant
    Filed: April 22, 2010
    Date of Patent: July 10, 2012
    Assignee: Abbott Laboratories
    Inventors: Gui-Dong Zhu, Virajkumar B. Gandhi, Jianchun Gong, Thomas D. Penning, Vincent L. Giranda, Sheela Thomas
  • Publication number: 20120172392
    Abstract: Compositions and methods are disclosed for inhibiting semicarbazide-sensitive amine oxidase (SSAO), also known as vascular adhesion protein-1 (VAP-1). The compounds disclosed are amine-containing and amide-containing compounds. The compounds and compositions are useful for treatment of diseases, including inflammation, inflammatory diseases and autoimmune disorders.
    Type: Application
    Filed: March 7, 2012
    Publication date: July 5, 2012
    Inventors: LUISA M. SALTER-CID, ERIC Y. WANG, MARY T. MACDONALD, JINGJING ZHAO
  • Patent number: 8202885
    Abstract: The invention relates to compounds of formula (I), wherein R1, R2, R1a, R2a, R3, R4, A, B, X, W and n are as defined in the description, and pharmaceutically acceptable salts of such compounds. These compounds are useful as calcium channel blockers.
    Type: Grant
    Filed: April 25, 2008
    Date of Patent: June 19, 2012
    Assignee: Actelion Pharmaceuticals Ltd.
    Inventors: Kurt Hilpert, Francis Hubler, Dorte Renneberg
  • Publication number: 20120122944
    Abstract: This invention relates to novel tetrahydronaphthalene derivatives, and pharmaceutically acceptable salts thereof according to the following formulae, in one embodiment: as described herein. This invention also provides compositions comprising a compound of this invention and the use of such compositions in methods of treating diseases and conditions that are beneficially treated by administering a selective T-type calcium channel blocker.
    Type: Application
    Filed: September 7, 2011
    Publication date: May 17, 2012
    Applicant: CONCERT PHARMACEUTICALS INC.
    Inventors: Roger Tung, Craig E. Masse, Bhaumik A. Pandya
  • Patent number: 8168668
    Abstract: The present invention relates to new compounds or salts, solvates or solvated salts thereof, processes for their preparation and to new intermediates used in the preparation thereof, pharmaceutical compositions containing said compounds and to the use of said compounds in therapy.
    Type: Grant
    Filed: October 14, 2009
    Date of Patent: May 1, 2012
    Assignee: AstraZeneca AB
    Inventors: Yevgeni Besidski, Martin Nylof, Inger Kers, Karin Skogholm, Shawn Johnstone, Paul Jones, Denis Labrecque, Andrew Griffin
  • Publication number: 20120101243
    Abstract: 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: Application
    Filed: December 19, 2011
    Publication date: April 26, 2012
    Inventors: W. Justin Youngblood, Jonathan S. Lindsey
  • Patent number: 8143282
    Abstract: The present invention relates to compounds which are inhibitors of histone deacetylase. More particularly, the present invention relates to heterocyclic compounds and methods for their preparation. These compounds may be useful as medicaments for the treatment of proliferative disorders as well as other diseases involving, relating to or associated with enzymes having histone deacetylase (HDAC) activities.
    Type: Grant
    Filed: August 1, 2006
    Date of Patent: March 27, 2012
    Assignee: S*BIO Pte Ltd.
    Inventors: Dizhong Chen, Weiping Deng, Ken C. Lee, Pek L. Lye, Eric T. Sun, Haishan Wang, Niefang Yu
  • Patent number: 8143422
    Abstract: The invention is concerned with novel benzimidazole derivatives of formula (I) wherein R1 to R6 are as defined in the description and in the claims, as well as physiologically acceptable salts and esters thereof. These compounds can be used as medicaments.
    Type: Grant
    Filed: October 13, 2009
    Date of Patent: March 27, 2012
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Gregory Martin Benson, Konrad Bleicher, Song Feng, Uwe Grether, Bernd Kuhn, Rainer E. Martin, Jean-Marc Plancher, Hans Richter, Sven Taylor
  • Publication number: 20120053188
    Abstract: The invention encompasses a compound derived from hydroxamic acid that may be used to slow the expansion of cancer cells and thus is effective in the treatment of cancer. Generally, the disclosed compound includes a benzimidazole group coupled to a hydroxyamide of five or more unsubstituted carbon atoms and any pharmaceutically acceptable salts, solvates and chemically protected forms thereof. Also disclosed are pharmacological compositions including the compound and methods of using the compound to slow the expansion of cancer cells as well as methods of using the compound to treat cancer.
    Type: Application
    Filed: February 3, 2009
    Publication date: March 1, 2012
    Applicant: THE TRANSLATIONAL GENOMICS RESEARCH INSTITUTE(TGEN
    Inventors: Tong Wang, Stephen Gately
  • Patent number: 8119675
    Abstract: Novel compounds of the formula I (I), in which R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R11, R12, R13, R, Q, W, X and Z have the meanings indicated in Patent Claim 1, are suitable as antidiabetics.
    Type: Grant
    Filed: January 28, 2008
    Date of Patent: February 21, 2012
    Assignee: Merck Patent GmbH
    Inventors: Lars Thore Burgdorf, Bertram Cezanne, Markus Klein, Rolf Gericke, Christos Tsaklakidis, Werner Mederski, Norbert Beier
  • Publication number: 20120040974
    Abstract: The invention provides novel heterocyclic compounds, pharmaceutical compositions and methods of treatment that modulate levels of MIF expression and treat disorders associated with high or low levels of MIF expression.
    Type: Application
    Filed: August 18, 2009
    Publication date: February 16, 2012
    Applicant: YALE UNIVERSITY
    Inventors: William L. Jorgensen, Richard J. Bucala
  • Publication number: 20120015998
    Abstract: Disclosed herein are compounds represented by a formula: R1—Ar1—X—Ar2—Ar3-Het, wherein R1, Ar1, X, Ar2, Ar3, and Het are described herein. Compositions and light-emitting devices related thereto are also disclosed.
    Type: Application
    Filed: July 11, 2011
    Publication date: January 19, 2012
    Applicant: Nitto Denko Corporation
    Inventors: Amane Mochizuki, Sazzadur Rahman Khan, Sheng Li, Shijun Zheng, Jensen Cayas, Keisaku Okada, Brett T. Harding
  • Patent number: 8093401
    Abstract: Provided herein are novel sirtuin-modulating compounds and methods of use thereof. The sirtuin-modulating compounds may be used for increasing the lifespan of a cell, and treating and/or preventing a wide variety of diseases and disorders including, for example, diseases or disorders related to aging or stress, diabetes, obesity, neurodegenerative diseases, cardiovascular disease, blood clotting disorders, inflammation, cancer, and/or flushing as well as diseases or disorders that would benefit from increased mitochondrial activity. Also provided are compositions comprising a sirtuin-modulating compound in combination with another therapeutic agent.
    Type: Grant
    Filed: August 4, 2006
    Date of Patent: January 10, 2012
    Assignee: Sirtris Pharmaceuticals, Inc.
    Inventors: Joseph J. Nunes, Jill Milne, Jean Bemis, Roger Xie, Chi B. Vu, Pui Yee Ng, Jeremy S. Disch
  • Patent number: 8093402
    Abstract: Provided herein are compounds in accord with Formula I: that are useful in the treatment of pain.
    Type: Grant
    Filed: February 8, 2011
    Date of Patent: January 10, 2012
    Assignee: AstraZeneca AB
    Inventors: William Brown, Shawn Johnstone, Denis Labrecque
  • Patent number: 8084484
    Abstract: Vanilloid receptor ligand compounds corresponding to formula I: pharmaceutical compositions containing such compounds, a process for producing such compounds, and methods of using such compounds for treating or inhibiting pain and various other disorders or conditions.
    Type: Grant
    Filed: April 15, 2008
    Date of Patent: December 27, 2011
    Assignee: Gruenenthal GmbH
    Inventors: Robert Frank, Gregor Bahrenberg, Thomas Christoph, Klaus Schiene, Jean De Vry, Derek Saunders, Bernd Sundermann, Jeewoo Lee
  • Publication number: 20110301192
    Abstract: The present invention provides compounds that inhibit cyclin kinase inhibitor p21, such as compounds of formula I. The present invention also provides compositions including compounds of Formula I and a pharmaceutically acceptable excipient. In addition, the present invention provides methods of inhibiting cyclin kinase inhibitor p21 and of treating cancer.
    Type: Application
    Filed: September 29, 2009
    Publication date: December 8, 2011
    Applicant: The regents of the University of California
    Inventors: Robert Weiss, See-Hyoung Park, Kit S. Lam, Ruiwu Liu
  • Publication number: 20110294804
    Abstract: The invention provides a compound for the treatment or prophylaxis of pathology involving SNS, specifically diseases such as neuropathic pain, nociceptive pain, dysuria, multiple sclerosis and the like.
    Type: Application
    Filed: December 25, 2009
    Publication date: December 1, 2011
    Applicant: DAINIPPON SUMITOMO PHARMA CO., LTD.
    Inventors: Katsunori Tsubio, Yusuke Yamai, Hitoshi Watanabe, Hironori Kinoshita
  • Publication number: 20110269706
    Abstract: The disclosure includes hydroxamic compounds of Formula I: (I) wherein P, Z, and m are defined herein. Also disclosed is a method for treating a neoplastic disease or an immune disease with these compounds.
    Type: Application
    Filed: January 7, 2010
    Publication date: November 3, 2011
    Applicant: Northlake Biosciences LLC
    Inventors: Yu Chen, Yi Chen
  • Publication number: 20110263648
    Abstract: The invention relates to compounds of formula (I) wherein R1, R2, R3, R4, A, B, W and n are as defined in the description, and to pharmaceutically acceptable salts of such compounds. These compounds are useful as calcium channel blockers.
    Type: Application
    Filed: October 21, 2009
    Publication date: October 27, 2011
    Inventors: Kurt Hilpert, Francis Hubler, Dorte Renneberg
  • Publication number: 20110263667
    Abstract: The invention relates to crystalline salts of isobutyric acid (1R*,2R*,4R*)-2-(2-{[3-(4,7-dimethoxy-1H-benzoimidazol-2-yl)-propyl]-methyl-amino}-ethyl)-5-phenyl-bicyclo[2.2.2]oct-5-en-2-yl ester, processes for the preparation thereof, pharmaceutical compositions containing said crystalline salts, and their use as medicaments, especially as calcium channel blockers.
    Type: Application
    Filed: October 21, 2009
    Publication date: October 27, 2011
    Inventors: Stefan Abele, Stéphanie Combes, Jacques-Alexis Funel, Kurt Hilpert, Francis Hubler, Katharina Reichenbaecher, Dorte Renneberg, Markus Von Raumer
  • Publication number: 20110237635
    Abstract: This invention relates to novel tetrahydronaphthalene derivatives, and pharmaceutically acceptable salts thereof according to the following formulae, in one embodiment: as described herein. This invention also provides compositions comprising a compound of this invention and the use of such compositions in methods of treating diseases and conditions that are beneficially treated by administering a selective T-type calcium channel blocker.
    Type: Application
    Filed: March 2, 2011
    Publication date: September 29, 2011
    Applicant: CONCERT PHARMACEUTICALS INC.
    Inventors: Roger Tung, Craig E. Masse
  • Patent number: 8008503
    Abstract: The invention is concerned with novel substituted benzimidazole derivatives of formula (I) wherein R1 to R10 are as defined in the description and in the claims, as well as physiologically acceptable salts and esters thereof. These compounds can be used as medicaments.
    Type: Grant
    Filed: August 25, 2010
    Date of Patent: August 30, 2011
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Gregory Martin Benson, Konrad Bleicher, Uwe Grether, Rainer E Martin, Jean-Marc Plancher, Hans Richter, Sven Taylor, Minmin Yang
  • Patent number: 8008335
    Abstract: The present invention relates to new indole and benzimidazole compounds and pharmaceutically acceptable salts, esters or prodrugs thereof, compositions of the new compounds together with pharmaceutically acceptable carriers, and uses of the new compounds. The compounds of the invention have the following general formula (I).
    Type: Grant
    Filed: October 14, 2005
    Date of Patent: August 30, 2011
    Assignee: Novartis Vaccines and Diagnostics, Inc.
    Inventors: Rustum S. Boyce, Yi Xia, Hongyan Guo, Kris G. Mendenhall, Annette O. Walter, Weibo Wang
  • Patent number: 8008305
    Abstract: The invention relates to a compound of formula wherein R1, R2, X, L, W, n, and o are defined herein and to pharmaceutically suitable acid addition salts thereof, with the exception of the following compounds 6-(4-methyl-piperazin-1-yl)-N-phenethyl-nicotinamide (CAS 199478-31-4), N-(3,4-dichloro-benzyl)-3-fluoro-benzamide (CAS 424815-98-5), N-(4-chloro-benzyl)-3-fluoro-benzamide (CAS 544661-83-8), N-(3-chloro-benzyl)-3-fluoro-benzamide (CAS 796051-07-5), and N-phenethyl-6-phenylamino-nicotinamide (CAS 571913-74-1). The compounds of formula I have a good affinity to the trace amine associated receptors (TAARs), especially for TAAR1 and are useful for the treatment of CNS disorders.
    Type: Grant
    Filed: July 28, 2008
    Date of Patent: August 30, 2011
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Guido Galley, Katrin Groebke Zbinden, Roger Norcross, Henri Stalder
  • Publication number: 20110207939
    Abstract: The present invention relates to novel inhibitors of Factors VIIa, IXa, Xa, XIa, in particular Factor VIIa, pharmaceutical compositions comprising these inhibitors, and methods for using these inhibitors for treating or preventing thromboembolic disorders, cancer or rheumatoid arthritis. Processes for preparing these inhibitors are also disclosed.
    Type: Application
    Filed: May 3, 2011
    Publication date: August 25, 2011
    Applicant: Pharmacyclics, Inc.
    Inventors: Daniel A. Dickman, Dange Vijay Kumar, Colin O'Bryan, Roopa Rai, William Dvorak Shrader, Kieron Wesson
  • Patent number: 7989472
    Abstract: Glucagon receptor antagonist compounds are disclosed. The compounds are useful for treating type 2 diabetes and related conditions. Pharmaceutical compositions and methods of treatment are also included.
    Type: Grant
    Filed: March 19, 2007
    Date of Patent: August 2, 2011
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Ronald M. Kim, Emma R. Parmee, Qiang Tan, Ashley Rouse Lins, Jiang Chang, Cangming Yang
  • Publication number: 20110137045
    Abstract: Provided herein are compounds in accord with Formula I: that are useful in the treatment of pain.
    Type: Application
    Filed: February 8, 2011
    Publication date: June 9, 2011
    Applicant: AstraZeneca AB
    Inventors: William Brown, Shawn Johnstone, Denis Labrecque
  • Patent number: 7935713
    Abstract: Glucagon receptor antagonist compounds are disclosed. The compounds are useful for treating type 2 diabetes and related conditions. Pharmaceutical compositions and methods of treatment are also included.
    Type: Grant
    Filed: May 11, 2007
    Date of Patent: May 3, 2011
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Ronald M. Kim, Emma R. Parmee, Qiang Tan, Cangming Yang, Ashley Rouse Lins
  • Patent number: 7928119
    Abstract: 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: Grant
    Filed: November 3, 2006
    Date of Patent: April 19, 2011
    Assignee: Pfizer Inc.
    Inventors: Masato Shimojo, Kana Taniguchi
  • Patent number: 7919510
    Abstract: The present invention relates to benzimidazole compounds having dual nitric oxide synthase (NOS) inhibitory activity and agonist activity at the mu-opioid receptor, to pharmaceutical and diagnostic compositions containing them, and to their medical use, particularly as compounds for the treatment or prevention of chronic pain, acute pain, migraine, and neuropathic pain.
    Type: Grant
    Filed: May 18, 2006
    Date of Patent: April 5, 2011
    Assignee: NeurAxon, Inc
    Inventors: Paul Renton, Shawn Maddaford, Suman Rakhit, John Andrews
  • Patent number: 7910228
    Abstract: The present invention provides for emissive materials comprising compounds of specific chemical structure, and electroluminescent devices comprising such emissive materials.
    Type: Grant
    Filed: November 14, 2008
    Date of Patent: March 22, 2011
    Assignee: Academia Sinica
    Inventors: Jiann T'suen Lin, Mei-Yi Lai, Chih-Hsin Chen
  • Patent number: 7906654
    Abstract: Provided herein are compounds in accord with Formula I: that are useful in the treatment of pain.
    Type: Grant
    Filed: August 9, 2007
    Date of Patent: March 15, 2011
    Assignee: AstraZeneca AB
    Inventors: William Brown, Shawn Johnstone, Denis Labrecque
  • Publication number: 20110059962
    Abstract: Substituted benzoimidazole compounds useful as anti-infectives that decrease resistance, virulence, or growth of microbes are provided. Methods of using substituted benzimidazole compounds, in, e.g., reducing virulence and infectivity, inhibiting biofilms and treating bacterial infections, are also provided.
    Type: Application
    Filed: April 22, 2010
    Publication date: March 10, 2011
    Inventors: MICHAEL N. ALEKSHUN, VICTORIA BARTLETT, MICHAEL P. DRAPER, LYNNE GARRITY-RYAN, RAINA GAY, MARK GRIER, OAK K. KIM, STUART B. LEVY
  • Publication number: 20110039905
    Abstract: The invention relates to compounds of formula (I) wherein R1 represents aryl, which is unsubstituted, or mono-, di-, or tri-substituted wherein the substituents are independently selected from the group consisting of (C1-4)alkyl, (C1-4)alkoxy, halogen, and trifluoromethyl; R2 represents hydrogen, or —CO—R21; R21 represents (C1-5)alkyl, (C1-3)fluoroalkyl, or (C3-6)cycloalkyl; m represents the integer 2, or 3; p represents the integer 2 or 3; and R3 represents hydrogen, or (C1-5)alkyl; and pharmaceutically acceptable salts of such compounds. These compounds are useful as calcium channel blockers.
    Type: Application
    Filed: April 23, 2009
    Publication date: February 17, 2011
    Inventors: Francis Hubler, Kurt Hilpert, Dorte Renneberg
  • Publication number: 20110033393
    Abstract: The present invention relates to hydrazone compounds of Formula I: and pharmaceutically acceptable salts and stereoisomers thereof, wherein R1, R2, R3, R4, L1, and L2 are defined as set forth in the specification. The invention is also directed to the use of compounds of Formula I as inhibitors of TRPM5 protein.
    Type: Application
    Filed: May 12, 2010
    Publication date: February 10, 2011
    Inventors: Philip STEIN, Robert DAINES, Dennis SPROUS, Harold O'GRADY
  • Patent number: 7884215
    Abstract: Inhibitors of RSV replication of formula (I) the addition salts and stereochemically isomeric forms thereof, wherein Q is hydrogen, C1-6alkyl optionally substituted with a heterocycle or Q is C1-6alkyl substituted with both —OR4 and a heterocycle; wherein said heterocycle is oxazolidine, thiazolidine, 1-oxo-thiazolidine, 1,1-dioxothiazolidine, morpholinyl, thiomorpholinyl, 1-oxo-thiomorpholinyl, 1,1-dioxothiomorpholinyl, hexahydrooxazepine, hexahydro-thiazepine, 1-oxo-hexahydrothiazepine, 1,1-dioxo-hexahydrothiazepine, pyrrolidine, piperidine, homopiperidine, piperazine; which heterocyle may be substituted with 1-2 substituents; each Alk is C1-6alkanediyl; R1 is Ar2 or optionally substituted piperidinyl, piperazinyl, morpholinyl, thiomorpholinyl, pyridyl, pyrazinyl, pyridazinyl, pyrimidinyl, furanyl, tetrahydro-furanyl, thienyl, pyrrolyl, thiazolyl, oxazolyl, imidazolyl, isothiazolyl, pyrazolyl, isoxazolyl, oxadiazolyl, quinolinyl, quinoxalinyl, benzofuranyl, benzothienyl, benzimidazolyl, benzoxazolyl, benzth
    Type: Grant
    Filed: June 20, 2006
    Date of Patent: February 8, 2011
    Inventors: Jean-François Bonfanti, Philippe Muller, Jérôme Michel Claude Fortin, Frédéric Marc Maurice Doublet
  • Patent number: 7880016
    Abstract: The invention relates to a process for preparing a salt of an optionally substituted 4-benzimidazol-2-ylmethylamino)-benzamidine, characterised in that (a) an optionally correspondingly substituted diaminobenzene is condensed with 2-[4-(1,2,4-oxadiazol-5-on-3-yl)-phenylamino]-acetic acid, b) i) the product thus obtained is hydrogenated, ii) optionally the amidino group is carbonylated, without isolating the intermediate product of the hydrogenation beforehand and iii) without prior isolation of the intermediate product of the carbonylation the desired salt is isolated.
    Type: Grant
    Filed: December 21, 2006
    Date of Patent: February 1, 2011
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Georg Zerban, Arndt Hausherr, Kerstin Schlarb, Rainer Hamm, Gunter Koch, Bjoern Weyell, Heinz-Peter Schmitt
  • Publication number: 20110020477
    Abstract: Wrinkles are improved by applying an oral preparation, injection preparation or external skin preparation having a substance that controls heparanase as an active ingredient thereof.
    Type: Application
    Filed: March 31, 2009
    Publication date: January 27, 2011
    Inventor: Shunsuke Iriyama
  • Publication number: 20100331371
    Abstract: The invention is concerned with novel substituted benzimidazole derivatives of formula (I) wherein R1 to R10 are as defined in the description and in the claims, as well as physiologically acceptable salts and esters thereof. These compounds can be used as medicaments.
    Type: Application
    Filed: August 25, 2010
    Publication date: December 30, 2010
    Inventors: Gregory Martin Benson, Konrad Bleicher, Uwe Grether, Rainer E. Martin, Jean-Marc Plancher, Hans Richter, Sven Taylor, Minmin Yang
  • Publication number: 20100324095
    Abstract: The present invention provides: a pharmaceutical composition for inhibiting amyloid-? protein accumulation comprising a compound of the formula (I) or a pharmaceutically acceptable salt thereof as an active ingredient; a method for inhibiting amyloid-? protein accumulation, comprising a step of administering an effective amount of the compound of the formula (I) or a pharmaceutically acceptable salt thereof to a mammal which may be diagnosed with an amyloid-? protein-related disease; and so on.
    Type: Application
    Filed: January 23, 2009
    Publication date: December 23, 2010
    Inventors: Kozo Motonaga, Koichi Saito, Koichiro Harada
  • Publication number: 20100286202
    Abstract: The present invention relates to new compounds or salts, solvates or solvated salts thereof, processes for their preparation and to new intermediates used in the preparation thereof, pharmaceutical compositions containing said compounds and to the use of said compounds in therapy.
    Type: Application
    Filed: October 14, 2009
    Publication date: November 11, 2010
    Applicant: AstraZeneca AB
    Inventors: Yevgeni Besidski, Martin Nylöf, Inger Kers, Karin Skogholm, Shawn Johnstone, Paul Jones, Denis Labrecque, Andrew Griffin
  • Patent number: 7825258
    Abstract: The invention is concerned with novel substituted benzimidazole derivatives of formula (I) wherein R1 to R10 are as defined in the description and in the claims, as well as physiologically acceptable salts and esters thereof. These compounds can be used as medicaments.
    Type: Grant
    Filed: November 5, 2008
    Date of Patent: November 2, 2010
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Gregory Martin Benson, Konrad Bleicher, Uwe Grether, Rainer E. Martin, Jean-Marc Plancher, Hans Richter, Sven Taylor, Minmin Yang