Nitrogen Attached Indirectly To The Diazole Ring By Acyclic Nonionic Bonding Patents (Class 548/309.7)
-
Publication number: 20130059852Abstract: 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: ApplicationFiled: April 8, 2011Publication date: March 7, 2013Applicant: UNIVERSITY OF LOUISVILLE RESEARCH FOUNDATION, INC.Inventors: John O. Trent, Jason B. Meier, Kelby B. Napier
-
Publication number: 20130029846Abstract: 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: ApplicationFiled: March 28, 2011Publication date: January 31, 2013Applicant: BASF SEInventors: Joachim Rheinheimer, Christian Pilger, Stefan Redlich, Doris Kremzow, Claudia Rosenbaum, Burghard Liebmann, Wassilios Grammenos
-
Publication number: 20130029964Abstract: 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: ApplicationFiled: August 27, 2012Publication date: January 31, 2013Applicant: DAIICHI SANKYO COMPANY, LIMITEDInventors: Kazumasa Aoki, Satoshi Matsui, Kenji Yoshikawa, Hiroki Shimizu, Junko Sasaki, Katsuyoshi Nakajima, Osamu Kanno, Kiyoshi Oizumi
-
Patent number: 8354543Abstract: 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: GrantFiled: April 29, 2010Date of Patent: January 15, 2013Assignee: Boehringer Ingelheim International GmbHInventors: Georg Zerban, Arndt Hausherr, Kerstin Schlarb, Rainer Hamm, Gunter Koch, Bjoem Weyell, Heinz-Peter Schmitt
-
Publication number: 20120330025Abstract: 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: ApplicationFiled: June 21, 2012Publication date: December 27, 2012Inventors: Harue Osaka, Takahiro Ushikubo, Tsunenori Suzuki, Nobuharu Ohsawa
-
Publication number: 20120316201Abstract: 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: ApplicationFiled: June 8, 2012Publication date: December 13, 2012Applicant: IPSEN PHARMA S.A.S.Inventors: Lÿdie POITOUT, Valerie Brault, Carole Sackur, Pierre Roubert, Pascale Plas
-
Patent number: 8314253Abstract: 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: GrantFiled: October 21, 2009Date of Patent: November 20, 2012Assignee: Actelion Pharmaceuticals Ltd.Inventors: Kurt Hilpert, Francis Hubler, Dorte Renneberg
-
Publication number: 20120184518Abstract: 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: ApplicationFiled: January 20, 2012Publication date: July 19, 2012Applicant: PROBIODRUG AGInventors: Stephan Schilling, Holger Cynis, Torsten Hoffman, Hans-Ulrich Demuth
-
Patent number: 8217070Abstract: 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: GrantFiled: April 22, 2010Date of Patent: July 10, 2012Assignee: Abbott LaboratoriesInventors: Gui-Dong Zhu, Virajkumar B. Gandhi, Jianchun Gong, Thomas D. Penning, Vincent L. Giranda, Sheela Thomas
-
Publication number: 20120172392Abstract: 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: ApplicationFiled: March 7, 2012Publication date: July 5, 2012Inventors: LUISA M. SALTER-CID, ERIC Y. WANG, MARY T. MACDONALD, JINGJING ZHAO
-
Patent number: 8202885Abstract: 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: GrantFiled: April 25, 2008Date of Patent: June 19, 2012Assignee: Actelion Pharmaceuticals Ltd.Inventors: Kurt Hilpert, Francis Hubler, Dorte Renneberg
-
Publication number: 20120122944Abstract: 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: ApplicationFiled: September 7, 2011Publication date: May 17, 2012Applicant: CONCERT PHARMACEUTICALS INC.Inventors: Roger Tung, Craig E. Masse, Bhaumik A. Pandya
-
Patent number: 8168668Abstract: 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: GrantFiled: October 14, 2009Date of Patent: May 1, 2012Assignee: AstraZeneca ABInventors: Yevgeni Besidski, Martin Nylof, Inger Kers, Karin Skogholm, Shawn Johnstone, Paul Jones, Denis Labrecque, Andrew Griffin
-
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
-
Patent number: 8143282Abstract: 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: GrantFiled: August 1, 2006Date of Patent: March 27, 2012Assignee: S*BIO Pte Ltd.Inventors: Dizhong Chen, Weiping Deng, Ken C. Lee, Pek L. Lye, Eric T. Sun, Haishan Wang, Niefang Yu
-
Patent number: 8143422Abstract: 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: GrantFiled: October 13, 2009Date of Patent: March 27, 2012Assignee: 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: 20120053188Abstract: 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: ApplicationFiled: February 3, 2009Publication date: March 1, 2012Applicant: THE TRANSLATIONAL GENOMICS RESEARCH INSTITUTE(TGENInventors: Tong Wang, Stephen Gately
-
Patent number: 8119675Abstract: 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: GrantFiled: January 28, 2008Date of Patent: February 21, 2012Assignee: Merck Patent GmbHInventors: Lars Thore Burgdorf, Bertram Cezanne, Markus Klein, Rolf Gericke, Christos Tsaklakidis, Werner Mederski, Norbert Beier
-
Publication number: 20120040974Abstract: 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: ApplicationFiled: August 18, 2009Publication date: February 16, 2012Applicant: YALE UNIVERSITYInventors: William L. Jorgensen, Richard J. Bucala
-
Publication number: 20120015998Abstract: 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: ApplicationFiled: July 11, 2011Publication date: January 19, 2012Applicant: Nitto Denko CorporationInventors: Amane Mochizuki, Sazzadur Rahman Khan, Sheng Li, Shijun Zheng, Jensen Cayas, Keisaku Okada, Brett T. Harding
-
Patent number: 8093401Abstract: 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: GrantFiled: August 4, 2006Date of Patent: January 10, 2012Assignee: Sirtris Pharmaceuticals, Inc.Inventors: Joseph J. Nunes, Jill Milne, Jean Bemis, Roger Xie, Chi B. Vu, Pui Yee Ng, Jeremy S. Disch
-
Patent number: 8093402Abstract: Provided herein are compounds in accord with Formula I: that are useful in the treatment of pain.Type: GrantFiled: February 8, 2011Date of Patent: January 10, 2012Assignee: AstraZeneca ABInventors: William Brown, Shawn Johnstone, Denis Labrecque
-
Patent number: 8084484Abstract: 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: GrantFiled: April 15, 2008Date of Patent: December 27, 2011Assignee: Gruenenthal GmbHInventors: Robert Frank, Gregor Bahrenberg, Thomas Christoph, Klaus Schiene, Jean De Vry, Derek Saunders, Bernd Sundermann, Jeewoo Lee
-
Publication number: 20110301192Abstract: 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: ApplicationFiled: September 29, 2009Publication date: December 8, 2011Applicant: The regents of the University of CaliforniaInventors: Robert Weiss, See-Hyoung Park, Kit S. Lam, Ruiwu Liu
-
Publication number: 20110294804Abstract: 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: ApplicationFiled: December 25, 2009Publication date: December 1, 2011Applicant: DAINIPPON SUMITOMO PHARMA CO., LTD.Inventors: Katsunori Tsubio, Yusuke Yamai, Hitoshi Watanabe, Hironori Kinoshita
-
Publication number: 20110269706Abstract: 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: ApplicationFiled: January 7, 2010Publication date: November 3, 2011Applicant: Northlake Biosciences LLCInventors: Yu Chen, Yi Chen
-
Publication number: 20110263648Abstract: 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: ApplicationFiled: October 21, 2009Publication date: October 27, 2011Inventors: Kurt Hilpert, Francis Hubler, Dorte Renneberg
-
Publication number: 20110263667Abstract: 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: ApplicationFiled: October 21, 2009Publication date: October 27, 2011Inventors: Stefan Abele, Stéphanie Combes, Jacques-Alexis Funel, Kurt Hilpert, Francis Hubler, Katharina Reichenbaecher, Dorte Renneberg, Markus Von Raumer
-
Publication number: 20110237635Abstract: 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: ApplicationFiled: March 2, 2011Publication date: September 29, 2011Applicant: CONCERT PHARMACEUTICALS INC.Inventors: Roger Tung, Craig E. Masse
-
Patent number: 8008503Abstract: 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: GrantFiled: August 25, 2010Date of Patent: August 30, 2011Assignee: 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: 8008335Abstract: 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: GrantFiled: October 14, 2005Date of Patent: August 30, 2011Assignee: Novartis Vaccines and Diagnostics, Inc.Inventors: Rustum S. Boyce, Yi Xia, Hongyan Guo, Kris G. Mendenhall, Annette O. Walter, Weibo Wang
-
Patent number: 8008305Abstract: 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: GrantFiled: July 28, 2008Date of Patent: August 30, 2011Assignee: Hoffmann-La Roche Inc.Inventors: Guido Galley, Katrin Groebke Zbinden, Roger Norcross, Henri Stalder
-
Publication number: 20110207939Abstract: 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: ApplicationFiled: May 3, 2011Publication date: August 25, 2011Applicant: Pharmacyclics, Inc.Inventors: Daniel A. Dickman, Dange Vijay Kumar, Colin O'Bryan, Roopa Rai, William Dvorak Shrader, Kieron Wesson
-
Patent number: 7989472Abstract: 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: GrantFiled: March 19, 2007Date of Patent: August 2, 2011Assignee: Merck Sharp & Dohme Corp.Inventors: Ronald M. Kim, Emma R. Parmee, Qiang Tan, Ashley Rouse Lins, Jiang Chang, Cangming Yang
-
Publication number: 20110137045Abstract: Provided herein are compounds in accord with Formula I: that are useful in the treatment of pain.Type: ApplicationFiled: February 8, 2011Publication date: June 9, 2011Applicant: AstraZeneca ABInventors: William Brown, Shawn Johnstone, Denis Labrecque
-
Patent number: 7935713Abstract: 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: GrantFiled: May 11, 2007Date of Patent: May 3, 2011Assignee: Merck Sharp & Dohme Corp.Inventors: Ronald M. Kim, Emma R. Parmee, Qiang Tan, Cangming Yang, Ashley Rouse Lins
-
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
-
Substituted benzimidazole compounds with dual NOS inhibitory activity and mu opioid agonist activity
Patent number: 7919510Abstract: 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: GrantFiled: May 18, 2006Date of Patent: April 5, 2011Assignee: NeurAxon, IncInventors: Paul Renton, Shawn Maddaford, Suman Rakhit, John Andrews -
Patent number: 7910228Abstract: The present invention provides for emissive materials comprising compounds of specific chemical structure, and electroluminescent devices comprising such emissive materials.Type: GrantFiled: November 14, 2008Date of Patent: March 22, 2011Assignee: Academia SinicaInventors: Jiann T'suen Lin, Mei-Yi Lai, Chih-Hsin Chen
-
Patent number: 7906654Abstract: Provided herein are compounds in accord with Formula I: that are useful in the treatment of pain.Type: GrantFiled: August 9, 2007Date of Patent: March 15, 2011Assignee: AstraZeneca ABInventors: William Brown, Shawn Johnstone, Denis Labrecque
-
Publication number: 20110059962Abstract: 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: ApplicationFiled: April 22, 2010Publication date: March 10, 2011Inventors: MICHAEL N. ALEKSHUN, VICTORIA BARTLETT, MICHAEL P. DRAPER, LYNNE GARRITY-RYAN, RAINA GAY, MARK GRIER, OAK K. KIM, STUART B. LEVY
-
Publication number: 20110039905Abstract: 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: ApplicationFiled: April 23, 2009Publication date: February 17, 2011Inventors: Francis Hubler, Kurt Hilpert, Dorte Renneberg
-
Publication number: 20110033393Abstract: 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: ApplicationFiled: May 12, 2010Publication date: February 10, 2011Inventors: Philip STEIN, Robert DAINES, Dennis SPROUS, Harold O'GRADY
-
Patent number: 7884215Abstract: 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, benzthType: GrantFiled: June 20, 2006Date of Patent: February 8, 2011Inventors: Jean-François Bonfanti, Philippe Muller, Jérôme Michel Claude Fortin, Frédéric Marc Maurice Doublet
-
Patent number: 7880016Abstract: 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: GrantFiled: December 21, 2006Date of Patent: February 1, 2011Assignee: Boehringer Ingelheim International GmbHInventors: Georg Zerban, Arndt Hausherr, Kerstin Schlarb, Rainer Hamm, Gunter Koch, Bjoern Weyell, Heinz-Peter Schmitt
-
Publication number: 20110020477Abstract: 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: ApplicationFiled: March 31, 2009Publication date: January 27, 2011Inventor: Shunsuke Iriyama
-
Publication number: 20100331371Abstract: 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: ApplicationFiled: August 25, 2010Publication date: December 30, 2010Inventors: Gregory Martin Benson, Konrad Bleicher, Uwe Grether, Rainer E. Martin, Jean-Marc Plancher, Hans Richter, Sven Taylor, Minmin Yang
-
Publication number: 20100324095Abstract: 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: ApplicationFiled: January 23, 2009Publication date: December 23, 2010Inventors: Kozo Motonaga, Koichi Saito, Koichiro Harada
-
Publication number: 20100286202Abstract: 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: ApplicationFiled: October 14, 2009Publication date: November 11, 2010Applicant: AstraZeneca ABInventors: Yevgeni Besidski, Martin Nylöf, Inger Kers, Karin Skogholm, Shawn Johnstone, Paul Jones, Denis Labrecque, Andrew Griffin
-
Patent number: 7825258Abstract: 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: GrantFiled: November 5, 2008Date of Patent: November 2, 2010Assignee: Hoffmann-La Roche Inc.Inventors: Gregory Martin Benson, Konrad Bleicher, Uwe Grether, Rainer E. Martin, Jean-Marc Plancher, Hans Richter, Sven Taylor, Minmin Yang