Bicyclo Ring System Which Is Benzimidazole (including Hydrogenated) Patents (Class 546/273.4)
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Publication number: 20100331323Abstract: The present invention provides active compounds for modulating nicotinic acetylcholine receptors and methods of making the same. The methods of preparing the active compounds utilize different intermediate compounds.Type: ApplicationFiled: September 10, 2010Publication date: December 30, 2010Inventors: Daniel L. Comins, Florence F. Wagner, Pauline Ondachi
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Publication number: 20100324298Abstract: A novel process for the preparation of omeprazole and its enantiomers, such as esomeprazole, as well as the preparation of related 2-(2-pyridinylmethyl-sulphinyl)-1H-benzimidazoles, including pantoprazole, lansoprazole and rabeprazole, as recemates or single enantiomers, and their alkali or alkaline salts has been developed. The novel process involves the surprising discovery that protection of the free-base benzimidazole sulfoxide (e.g. omeprazole or esomeprazole), by reaction with an alkyl, aryl or aralkyl chloroformate following oxidation of the corresponding sulfide, eliminates the need for its direct isolation. Subsequent removal of the protecting group with a solution of alkali or alkaline earth alkoxide in a C1-C4 alcohol directly provides the corresponding salt. By eliminating the need to handle the free-base benzimidazole sulfoxide, this advantageous procedure provides increased chemical yields over processes described in the art.Type: ApplicationFiled: August 12, 2010Publication date: December 23, 2010Applicant: APOTEX PHARMACHEM INC.Inventors: Fan Wang, Laura Kaye Montemayor, Daqing Che, Stephen E. Horne
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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
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Publication number: 20100324058Abstract: This invention relates to new chemical compounds, application of these compound as thrombin inhibitors, and pharmaceutical compositions based on them, and can be used to treat and prevent thrombin-dependent thromboembolic events, and in research.Type: ApplicationFiled: June 27, 2008Publication date: December 23, 2010Applicant: Obschestvo S Organichennoi Otvetsttvennoctiyou "Bionika"Inventors: Elena Ivanovna Sinauridze, Fazoil Inoyatovich Ataullakhanov, Andrey Alexandrovich Butylin, Vladimir Borisovich Sulimov, Alexey Nickolayevich Romanov, Alexey Alexeevich Bogolyubov, Yury Vladimirovich Kuznetsov, Irina Vladimirovna Gribkova, Alexander Sergeevich Gorbatenko, Olga Anatolievna Kondakova
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Publication number: 20100316607Abstract: The present invention discloses compounds of Formula (I), or pharmaceutically acceptable salts, esters, or prodrugs thereof: which inhibit RNA-containing virus, particularly the hepatitis C virus (HCV). Consequently, the compounds of the present invention interfere with the life cycle of the hepatitis C virus and are also useful as antiviral agents. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from HCV infection. The invention also relates to methods of treating an HCV infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention.Type: ApplicationFiled: June 15, 2010Publication date: December 16, 2010Inventors: Yat Sun Or, Xiaowen Peng, Lu Ying, Ce Wang, Yao-Ling Qiu
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Publication number: 20100317660Abstract: The present invention makes available methods and reagents for inhibiting aberrant growth states resulting from hedgehog gain-of-function, ptc loss-of-function or smoothened gain-of-function comprising contacting the cell with a hedgehog antagonist of formula (I) in a sufficient amount to aberrant growth state, e.g., to agonize a normal ptc pathway or antagonize smoothened or hedgehog activity.Type: ApplicationFiled: August 2, 2010Publication date: December 16, 2010Inventors: Oivin M. Guicherit, Edward Andrew Boyd, Judith Boyd, Shirley Ann Brunton, Stephen Price, John Harry Alexander Stibbard, Colin H. Mackinnon
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Patent number: 7851490Abstract: This invention relates to novel benzimidazole derivatives, pharmaceutical compositions containing these compounds, and methods of treatment therewith. The compounds of the invention are useful in the treatment of central nervous system diseases and disorders, which are responsive to modulation of the GABAA receptor complex, and in particular for combating anxiety and related diseases.Type: GrantFiled: April 7, 2006Date of Patent: December 14, 2010Assignee: Neurosearch A/SInventors: Janus S. Larsen, Lene Teuber, Philip K. Ahring, Elsebet Østergaard Nielsen, Naheed Mirza
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Patent number: 7851701Abstract: A photoelectric conversion device using a semiconductor fine material such as a semiconductor fine particle sensitized with a dye carried thereon, characterized in that the dye is a methine type dye having a specific partial structure, for example, a methine type dye having a specific carboxyl-substituted hetero ring on one side of a methine group and an aromatic residue substituted with a dialkylamino group or an organic metal complex residue on the other side of the methine group, or a methine type dye having a carboxyl-substituted aromatic ring on one side of a methine group and a heteroaromatic ring having a dialkylamino group or an organic metal complex residue on the other side of the methine group; and a solar cell using the photoelectric conversion element. The photoelectric conversion element exhibits a conversion efficiency comparable or superior to that of a conventionally known photoelectric conversion element sensitized with a methine type dye.Type: GrantFiled: July 5, 2002Date of Patent: December 14, 2010Assignee: Nippon Kayaku Kabushiki KaishaInventors: Masaaki Ikeda, Koichiro Shigaki, Teruhisa Inoue
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Patent number: 7851071Abstract: A novel derivative of heterocyclic compound having nitrogen atom with a structure made by bonding special groups to benzimidazole, a material for an organic electroluminescence (EL) device comprising the derivative of heterocyclic compound having nitrogen atom and an organic electroluminescence device comprising at least one organic compound layer containing a light emitting layer sandwiched between a pair of electrodes, wherein the device contains the derivative of heterocyclic compound having nitrogen atom. An organic EL device achieving elevation of luminance and of efficiency in light emission even under low driving voltage is obtainable by an employment of the derivative of heterocyclic compound having nitrogen atom for at least one layer composing organic compound layers of the EL device.Type: GrantFiled: January 27, 2004Date of Patent: December 14, 2010Assignee: Idemitsu Kosan Co., Ltd.Inventors: Hiroshi Yamamoto, Masahide Matsuura, Mineyuki Kubota, Masahiro Kawamura
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Publication number: 20100311748Abstract: The present disclosure relates to heterocyclic amide compounds, which are useful for inhibiting the Hedgehog pathway, and their use in treating a disease or medical condition mediated alone or in part by Hedgehog pathway inhibition. Also disclosed are methods for manufacture of these compounds, pharmaceutical compositions including these compounds, and use of these compounds in the manufacture of medicaments for treating such diseases and medical conditions in a subject. Formula (IA) with the provisio that either R2 or R3 is (Z).Type: ApplicationFiled: August 29, 2008Publication date: December 9, 2010Applicant: ASTRAZENECA ABInventors: Leslie Dakin, Benjamin Fauber, Alexander Hird, James Janetka, Daniel John Russell, Qibin Su, Bin Yang, Xiaolan Zheng
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Publication number: 20100298321Abstract: Disclosed are compounds which inhibit the activity of anti-apoptotic Bcl-2 or Bcl-xL proteins, compositions containing the compounds and methods of treating diseases during which are expressed anti-apoptotic Bcl-2 protein.Type: ApplicationFiled: June 3, 2010Publication date: November 25, 2010Applicant: ABBOTT LABORATORIESInventors: Milan Bruncko, Hong Ding, George A. Doherty, Steven W. Elmore, Lisa Hasvold, Laura Hexamer, Aaron R. Kunzer, Robert A. Mantei, William J. McClellan, Chang H. Park, Cheol-Min Park, Andrew M. Petros, Xiaohong Song, Andrew J. Souers, Gerard M. Sullivan, Zhi-Fu Tao, Gary T. Wang, Le Wang, Xilu Wang, Michael D. Wendt, Todd M. Hansen
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Publication number: 20100292276Abstract: The present invention is directed to benzimidazole derivatives, pharmaceutical compositions containing them and their use in the treatment of disorders and conditions modulated by TRP M8 (transient receptor potential M8 channel). More particularly, the compounds of the present invention are useful in the treatment of inflammatory pain, inflammatory hyperalgesia, inflammatory hypersensitivity condition, neuropathic pain, neuropathic cold allodynia, inflammatory somatic hyperalgesia, inflammatory visceral hyperalgesia, cardiovascular disease aggravated by cold, anxiety and depression.Type: ApplicationFiled: May 4, 2010Publication date: November 18, 2010Inventors: Raul R. Calvo, Sanath K. Meegalla, Mark R. Player
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Publication number: 20100286190Abstract: Certain chemical entities chosen from compounds of Formula 1 and pharmaceutically acceptable salts, solvates, chelates, non-covalent complexes, and prodrugs thereof, are provided herein. Pharmaceutical compositions comprising at least one chemical entity and one or more pharmaceutically acceptable vehicles chosen from carriers, adjuvants, and excipients, are also provided herein. Methods of treating patients suffering from certain diseases and disorders responsive to angiogenic kinase modulation, which comprise administering to such patients an amount of at least one chemical entity effective to reduce signs or symptoms of the disease or disorder are disclosed. These diseases include cancer, including breast neoplasia, endometrial cancer, colon cancer, and neck squamous cell carcinoma. Methods of treatment include administering at least one chemical entity as a single active agent or administering such at least one chemical entity in combination with one or more other therapeutic agents.Type: ApplicationFiled: July 20, 2010Publication date: November 11, 2010Inventors: Scott A. Mitchell, Mihaela Diana Danca, Peter A. Blomgren, David R. Brittelli, Pavel Zhichkin, Matthew E. Voss
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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
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Publication number: 20100280012Abstract: An azaazulene compound is provided. The azaazulene compound has formula (I) shown below. Each variable in formula (I) is defined in the specification. The compound can be used to treat cancer. The invention also provides a method for treating cancer. The method includes administering to a subject in need thereof an effective amount of one or more azaazulene compounds of formula (I).Type: ApplicationFiled: April 28, 2010Publication date: November 4, 2010Applicant: INDUSTRIAL TECHNOLOGY RESEARCH INSTITUTEInventor: On LEE
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Publication number: 20100273831Abstract: The present invention is related to novel benzimidazole compounds of formula (I) having cannabinoid receptor agonistic properties, pharmaceutical compositions comprising these compounds, chemical processes for preparing these compounds and their use in the treatment of diseases linked to the mediation of the cannabinoid receptors in animals, in particular humans.Type: ApplicationFiled: December 16, 2008Publication date: October 28, 2010Inventors: Henricus Jacobus Maria Gijsen, Bie Maria Pieter Verbist, Michel Surkyn
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Publication number: 20100273830Abstract: An insecticidal compound of formula (I) in which G1, G2, and G3 together with the two carbon atoms to which G1 and G3 are attached, form a non-aromatic 4- or 5-membered ring system; wherein G1 is sulfur, SO, SO2, oxygen, a direct bond, NRa or CR5aR5b; G2 is sulfur, SO, SO2, oxygen, a direct bond, NRb or CR5cR5d; G3 is sulfur, SO, SO2, oxygen, a direct bond, NRc or CR5eR5f; with the provisos that a) not more than 1 group G can be a direct bond, b) not more than 2 G groups can be oxygen, sulfur, SO or SO2 and c) when 2 G groups are oxygen, SO, SO2 and/or sulfur the two groups are separated by a carbon atom; each of Z1 and Z2, which may be the same or different, represents oxygen or sulfur; D is phenyl or a 5- or 6-membered heteroaromatic ring and R1a, R1b, R5a, R5b, R5c, R5d, R5e, R5f, Ra, Rb Rc, R2, R3 and R20 are specified organic groups and agronomically acceptable salts/isomers/enantiomers/tautomers/N-oxides of those compounds.Type: ApplicationFiled: July 14, 2008Publication date: October 28, 2010Applicant: SYNGENTA CROP PROTECTION, INC.Inventors: Roger Graham Hall, Olivier Loiseleur, Jagadish Pabba, Sitaram Pal, Andre Jeanguenat, Andrew Edmunds, Andre Stoller
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Publication number: 20100267698Abstract: This invention relates to benzimidazoles, pyridylimidazoles and related bicyclic heteroaryl compounds, all of which may be described by of Formula I The invention is particularly related to such compounds that bind with high selectivity and high affinity to the benzodiazepine site of GABAA receptors. This invention also relates to pharmaceutical compositions comprising such compounds and to the use of such compounds in treatment of certain central nervous system (CNS) diseases. Novel processes for preparing compounds of Formula I are disclosed. This invention also relates to the use of benzimidazoles, pyridylimidazoles and related bicyclic heteroaryl compounds of Formula I in combination with one or more other CNS agents to potentiate the effects of the other CNS agents. Additionally this invention relates to the use such compounds as probes for the localization of GABAA receptors in tissue sections.Type: ApplicationFiled: January 5, 2010Publication date: October 21, 2010Inventors: Guiying Li, Pamela Albaugh, Kevin S. Currie, Guolin Cai, Linda M. Gustavson, Kyungae Lee, Alan Hutchison, George D. Maynard, Jun Yuan, Ling Hong Xie, Manuka Ghosh, Nian Liu, George P. Luke, Scott Mitchell, Martin Patrick Allen, Spiros Liras
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Publication number: 20100267710Abstract: Disclosed are compounds of the Formula I and pharmaceutically acceptable salts and prodrugs thereof, wherein W, R1, R2, R7, R8, R9 and R10 are as defined in the specification. Such compounds are MEK inhibitors and useful in the treatment of hyperproliferative diseases, such as cancer and inflammation, in mammals. Also disclosed is a method of using such compounds in the treatment of hyperproliferative diseases in mammals, and pharmaceutical compositions containing such compounds.Type: ApplicationFiled: June 28, 2010Publication date: October 21, 2010Applicant: ARRAY BIOPHARMA INC.Inventors: Eli M. Wallace, Joseph P. Lyssikatos, Allison L. Marlow, T. Brian Hurley
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Patent number: 7816369Abstract: The present invention makes available methods and reagents for inhibiting aberrant growth states resulting from hedgehog gain-of-function, ptc loss-of-function or smoothened gain-of-function comprising contacting the cell with a hedgehog antagonist, such as a small molecule, in a sufficient amount to aberrant growth state, e.g., to agonize a normal ptc pathway or antagonize smoothened or hedgehog activity.Type: GrantFiled: November 3, 2005Date of Patent: October 19, 2010Assignees: Curis, Inc., Genentech, Inc.Inventors: Oivin M. Guicherit, Edward Andrew Boyd, Judith Boyd, legal representative, Shirley Ann Brunton, Stephen Price, John Harry Alexander Stibbard, Colin H. MacKinnon
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Publication number: 20100261717Abstract: Disclosed are compounds of the Formula I and pharmaceutically acceptable salts and prodrugs thereof, wherein W, R1, R2, R7, R8, R9 and R10 are as defined in the specification. Such compounds are MEK inhibitors and useful in the treatment of hyperproliferative diseases, such as cancer and inflammation, in mammals. Also disclosed is a method of using such compounds in the treatment of hyperproliferative diseases in mammals, and pharmaceutical compositions containing such compounds.Type: ApplicationFiled: June 28, 2010Publication date: October 14, 2010Applicant: ARRAY BIOPHARMA INC.Inventors: Eli M. Wallace, Joseph P. Lyssikatos, Allison L. Marlow, T. Brian Hurley
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Publication number: 20100261909Abstract: The present invention relates to a process for the regioselective synthesis of compounds of the formula I, wherein R0; R1; R2; R3; R4; R5; A1; A2; A3; A4, Q and J have the meanings indicated in the claims. The present invention provides a direct 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: October 14, 2010Applicant: sanofi-aventisInventors: Jorge ALONSO, Andreas LINDENSCHMIDT, Marc NAZARÉ, Matthias URMANN, Nis HALLAND, Omar RKYEK
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Patent number: 7812251Abstract: A photosensitizing transition metal complex of the formula (Ia) MLY1, (Ib) MLX3 (Ic) MLY2X, (Id) MLY3X or (Ie) MLY4X in which M is a transition metal selected from ruthenium, osmium, iron, rhenium and technetium, preferably ruthenium or osmium. X is a co-ligand independently selected from NCS—, Cl—, Br—, I—, CN—, H2O; pyridine unsubstituted or substituted by at least one group selected from vinyl, primary, secondary or tertiary amine, OH and C1-30 alkyl, preferably NSC and CN—; L is a tridentate polypyridine ligand, carrying at least one carboxylic, phosphoric acid or a chelating group and one substituted or unsubstituted alkyl group having 1 to 50 carbon atoms, substituted or unsubstituted alkylamide group having 2 to 30 carbon atoms or substituted or unsubstituted aralkyl group having 7 to 50 carbon atoms.Type: GrantFiled: October 15, 2004Date of Patent: October 12, 2010Assignee: Sharp Kabushiki KaishaInventors: Ashraful Islam, Liyuan Han, Atsushi Fukui
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Publication number: 20100256375Abstract: Methods for preparing new substituted benzimidazole compounds having formula (I) useful for treating kinase mediated disorders are provided wherein R1, R2, R3, R4, a, b, and c are defined hereinType: ApplicationFiled: June 18, 2010Publication date: October 7, 2010Inventors: Martin Dimitroff, Bridget R. Miller, Brady S. Stillwell, David A. Siesel, Tyson Swiftney, Brian Diaz, Danlin Gu, Jonathan P. van Dyck, David Ryckman, Daniel J. Poon, Teresa E. Pick
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Publication number: 20100256188Abstract: The present invention relates to compounds of general formula I in which A, L, M, Q2, Q3, Q4, R1, R5, Ra, Rb, Rc, W, X, Y, Z1, Z2, Z3 are defined in the description, the salts thereof, particularly the physiologically acceptable salts thereof. The compounds are of potential utility in the treatment and/or prevention of inflammatory diseases and associated conditions, in particular, in the treatment and/or prevention of pain. The invention also relates to the use of such compounds as medicaments, to pharmaceutical compositions containing them, and to their preparation.Type: ApplicationFiled: March 4, 2010Publication date: October 7, 2010Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Roland PFAU, Kirsten ARNDT, Henri DOODS, Klaus KLINDER, Raimund KUELZER, Dimitrijs LUBRIKS, Juergen MACK, Benjamin PELCMAN, Henning PRIEPKE, Robert ROENN, Dirk STENKAMP, Edgars SUNA
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Patent number: 7807697Abstract: Compounds of formula (I) are useful in treating conditions or disorders prevented by or ameliorated by histamine-3 receptor ligands. Also disclosed are pharmaceutical compositions comprising the histamine-3 receptor ligands and methods for using such compounds and compositions.Type: GrantFiled: January 29, 2008Date of Patent: October 5, 2010Assignee: Abbott LaboratoriesInventors: Marlon D. Cowart, Yi-Yin Ku, Sou-Jen Chang, Dilinie P. Fernando, Timothy A. Grieme, Robert J. Altenbach
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Publication number: 20100240580Abstract: The invention relates to azoloarine derivatives of formula I wherein R, A, B, D, Y, X, M and W are as defined herein, and their physiologically tolerated salts.Type: ApplicationFiled: February 18, 2010Publication date: September 23, 2010Applicant: SANOFI-AVENTISInventors: Gerhard ZOLLER, Marc Dietrich VOSS, Hans MATTER, Andreas HERLING, Christophe Philippo, Claudie NAMANE, Juan-Antonio SANCHEZ-ARIAS
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Publication number: 20100234425Abstract: 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: ApplicationFiled: April 22, 2010Publication date: September 16, 2010Applicant: ABBOTT LABORATORIESInventors: Gui-Dong Zhu, Virajkumar B. Gandhi, Jianchun Gong, Thomas D. Penning, Vincent L. Giranda, Sheela Thomas
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Publication number: 20100234394Abstract: New substituted benzimidazole compounds, compositions, and methods of inhibition of kinase activity associated with tumorigenesis in a human or animal subject are provided. In certain embodiments, the compounds and compositions are effective to inhibit the activity of at least one serine/threonine kinase or receptor tyrosine kinase. The new compounds and compositions may be used either alone or in combination with at least one additional agent for the treatment of a serine/threonine kinase- or receptor tyrosine kinase-mediated disorder, such as cancer.Type: ApplicationFiled: April 13, 2010Publication date: September 16, 2010Inventors: Mina E. Aikawa, Payman Amiri, Jeffrey H. Dove, Barry Haskell Levine, Christopher McBride, Teresa E. Pick, Daniel J. Poon, Savithri Ramurthy, Paul A. Renhowe, Cynthia Shafer, Darrin Stuart, Sharadha Subramanian
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Publication number: 20100227889Abstract: A compound of formula (I) or a pharmaceutically acceptable salt or prodrug ester thereof: wherein R, X and Y are as disclosed in the specification, suitable for the treatment of osteoporosis.Type: ApplicationFiled: March 28, 2007Publication date: September 9, 2010Inventors: Marc Gerspacher, Karl Heinz Krawinkler
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Publication number: 20100222345Abstract: This invention relates to novel compounds which are antagonists or inverse agonists at one or more of the opioid receptors, to pharmaceutical compositions containing them, to processes for their preparation, and to their use in therapy.Type: ApplicationFiled: August 8, 2007Publication date: September 2, 2010Inventors: Caroline Jean Diaz, Curt Dale Haffner, Jason Daniel Speake, Cunyu Zhang, Wendy Yoon Mills, Paul Kenneth Spearing, David John Cowan, Gary Martin Green
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Publication number: 20100216844Abstract: The present invention relates to novel carboxamide compounds and their use as a medicament. The carboxamide compounds are inhibitors of calpain (calcium dependant cysteine proteases). The invention therefore also relates to the use of these carboxamide compounds for treating a disorder associated with an elevated calpain activity and to a method for the therapeutic and/or prophylactic treatment by administering an effective amount of at least one of these carboxamide compounds. The carboxamide compounds are compounds of the general formula I in which W—R2 is selected from and R1, R2, R3a, R3b, Y1, Y2, Y3, Y4, X, Q, m, k, Rw and Rw* have the meanings mentioned in the claims, the tautomers thereof and the pharmaceutically suitable salts thereof.Type: ApplicationFiled: February 19, 2010Publication date: August 26, 2010Inventors: Andreas Kling, Helmul Mack, Kaija Junios, Achim Mceller, Wllirled Hombarger, Charles W. Hulchins
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Patent number: 7781595Abstract: The present invention relates to hydroxamate compounds which are inhibitors of histone deacetylase. More particularly, the present invention relates to benzimidazole containing 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 dysregulation of histone deacetylase (HDAC).Type: GrantFiled: September 21, 2004Date of Patent: August 24, 2010Assignee: S*BIO Pte Ltd.Inventors: DiZhong Chen, Hong Yan Song, Eric T. Sun, Niefang Yu, Yong Zou
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Publication number: 20100209418Abstract: The present invention is directed to solid forms of the Raf kinase inhibitor 1-methyl-5-(2-(5-(trifluoromethyl)-1H-imidazol-2-yl)pyridin-4-yloxy)-N-(4-(trifluoromethyl)phenyl)-1H-benzo[d]imidazol-2-amine, as well as compositions thereof and uses of the same.Type: ApplicationFiled: February 28, 2008Publication date: August 19, 2010Inventors: Ahmad Hashash, Kangwen L. Lin, Augustus O. Okhamafe
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Publication number: 20100210845Abstract: The invention relates to a process for preparing 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 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: ApplicationFiled: April 29, 2010Publication date: August 19, 2010Applicant: BOERINGER INGELHEIM INTERNATIONAL GMBHInventors: Georg ZERBAN, Arndt HAUSHERR, Kerstin SCHLARB, Rainer HAMM, Gunter KOCH, Bjoem WEYELL, Heinz-Peter SCHMITT
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Patent number: 7776900Abstract: This invention relates to novel benzimidazole derivatives, pharmaceutical compositions containing these compounds, and methods of treatment therewith. The compounds of the invention are useful in the treatment of central nervous system diseases and disorders, which are responsive to modulation of the GABAA receptor complex, and in particular for combating anxiety and related diseases.Type: GrantFiled: April 18, 2006Date of Patent: August 17, 2010Assignee: Neurosearch A/SInventors: Lene Teuber, Janus S. Larsen, Philip K. Ahring, Elsebet Østergaard Nielsen, Naheed Mirza
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Publication number: 20100197652Abstract: The present invention is directed to pyridyl carboxamide compounds which are antagonists of orexin receptors, and which are useful in the treatment or prevention of neurological and psychiatric disorders and diseases in which orexin receptors are involved. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which orexin receptors are involved.Type: ApplicationFiled: August 7, 2008Publication date: August 5, 2010Inventors: Jeffrey M. Bergman, Paul J. Coleman, Mark E. Fraley, Swati P. Mercer, Thomas S. Reger, Anthony J. Roecker, Justin T. Steen
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Publication number: 20100193773Abstract: A novel derivative of heterocyclic compound having nitrogen atom with a structure made by bonding special groups to benzimidazole, a material for an organic electroluminescence (EL) device comprising the derivative of heterocyclic compound having nitrogen atom and an organic electroluminescence device comprising at least one organic compound layer containing a light emitting layer sandwiched between a pair of electrodes, wherein the device contains the derivative of heterocyclic compound having nitrogen atom. An organic EL device achieving elevation of luminance and of efficiency in light emission even under low driving voltage is obtainable by an employment of the derivative of heterocyclic compound having nitrogen atom for at least one layer composing organic compound layers of the EL device.Type: ApplicationFiled: April 7, 2010Publication date: August 5, 2010Applicant: Idemitsu Kosan Co., Ltd,Inventors: Hiroshi Yamamoto, Masahide Matsuura, Mineyuki Kubota, Masahiro Kawamura
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Publication number: 20100197871Abstract: Ligands useful for promoting copper-catalyzed azide-alkyne cycloaddition reactions comprise a compound represented by structural Formula (I) as described in the specification, wherein in Formula (I) Z1 is a nitrogen-containing heterocyclic group or a group represented by the formula: Y1—(CH2)c—Y2—(CH2)d—Y3—CH2—N(CH2Z4)(CH2Z5), where Y1 is -E1-C(O)O—, -E1-C(O)NH—, -E1-, or a covalent bond; Y2 is a covalent bond, —CH?CH—, or a 1,4-(1,2,3-triazolyl) group; Y3 is —OC(O)-E2-, —NHC(O)-E2-, -E2-, or a covalent bond; each of E1 and E2 is a benzimidazolyl group attached at the 1 and 2 positions; each of c and d is independently 1, 2, 3, 4, or 5; each of Z2, Z3, Z4 and Z5 is a nitrogen-containing heterocyclic group including a substituent X1 and optionally including a substituent (CH2)n—R1, and Y1, Y2, Y3, X1, R1, c, d and n are each as defined in the specification.Type: ApplicationFiled: September 15, 2008Publication date: August 5, 2010Inventors: M.G. Finn, Valentin O. Rodionov
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Publication number: 20100196368Abstract: New substituted benz-azole compounds, compositions and methods of inhibition of Raf kinase activity in a human or animal subject are provided. The new compounds compositions may be used either alone or in combination with at least one additional agent for the treatment of a Raf kinase mediated disorder, such as cancer.Type: ApplicationFiled: March 12, 2010Publication date: August 5, 2010Applicant: NOVARTIS VACCINES AND DIAGNOSTICS, INC.Inventors: Payman Amiri, Wendy Fantl, Teresa Hansen, Barry Haskell Levine, Christopher McBride, Daniel J. Poon, Savithri Ramurthy, Paul A. Renhowe, Cynthia M. Shafer, Sharadha Subramanian, Leonard Sung
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Patent number: 7767820Abstract: Methods for preparing new substituted benzimidazole compounds having formula (I) useful for treating kinase mediated disorders are provided wherein R1, R2, R3, R4, a, b, and c are defined hereinType: GrantFiled: May 5, 2008Date of Patent: August 3, 2010Assignee: Novartis Vaccines and Diagnostics, Inc.Inventors: Martin Dimitroff, Bridget R. Miller, Brady S. Stillwell, David A. Siesel, Tyson Swiftney, Brian Diaz, Danlin Gu, Jonathan P. Van Dyck, David Ryckman, Daniel J. Poon, Teresa E. Pick
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Publication number: 20100184747Abstract: The present invention encompasses compounds of general formula (1) wherein R1 to R4 are defined as in claim 1, which are suitable for the treatment of diseases characterised by excessive or abnormal cell proliferation, and their use for preparing a pharmaceutical composition having the above-mentioned properties.Type: ApplicationFiled: June 9, 2008Publication date: July 22, 2010Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Matthias Treu, Ulrich Guertler, Thomas Karner, Oliver Kraemer, Jens Juergen Quant, Stephan Karl Zahn
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Publication number: 20100179147Abstract: Benzimidazole compounds of formula (I): wherein R1, R2, R3, R4, R5, X, Y, Z1, and Z2 are defined herein. Also disclosed is a method for treating cancer with benzimidazole compounds.Type: ApplicationFiled: December 10, 2009Publication date: July 15, 2010Inventors: Chih-Shiang Chang, Jih-Hwa Guh, Che-Ming Teng, Shiow-Lin Pan, Wei-Ling Chang, Ju-Fang Liu, Kai-Wei Chang, Sheng-Chu Kuo
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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: 20100173946Abstract: Compounds useful as GnRH receptor antagonists are provided. The present inventors have further examined propane-1,3-dione derivatives and confirmed as a result that a propane-1,3-dione having 2-(1,3-dihydro-2H-benzimidazol-2-ylidene), or a compound which has benzene or thiophene ring substituted with a group derived from 1-hydroxymethyl, shows excellent availability, in addition to its excellent GnRH receptor antagonism, thereby accomplishing the invention. Since the compound of the invention shows excellent availability, in addition to its strong GnRH receptor antagonism, it can be expected that it exerts superior drug effect in the living body, and it is useful for the treatment of sex hormone dependent diseases such as prostate cancer, breast cancer, endometriosis, uterine leiomyoma, benign prostatic hypertrophy and the like.Type: ApplicationFiled: March 18, 2010Publication date: July 8, 2010Applicant: ASTELLAS PHARMA INCInventors: Masaaki Hirano, Eiji Kawaminami, Isao Kinoyama, Shunichiro Matsumoto, Kei Ohnuki, Kazuyoshi Obitsu, Toshiyuki Kusayama
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Publication number: 20100168060Abstract: Salts of benzimidazolyl pyridyl ethers are provided, particularly salts of {1-methyl-5-[2-(5-trifluoromethyl-1H-imidazol-2-yl)-pyridin-4-yloxy]-1H-benzoimidazol-2-yl}-(4-trifluoromethyl-phenyl)amine. Compositions and formulations including such salts and surfactants as well as methods of preparing such compositions and formulations are provided.Type: ApplicationFiled: August 30, 2007Publication date: July 1, 2010Applicant: Novartis AGInventors: Rampurna Gullapalli, Ahmad Hashash, Piotr H. Karpinski, Kangwen L. Lin, Eric M. Loeser, Augustus O. Okhamafe, Paul Allen Sutton, Eduardo Sy
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Publication number: 20100168181Abstract: Objects of the present invention are the compounds of formula (I) their pharmaceutically acceptable salts, enantiomeric forms, diastereoisomers and racemates, the preparation of the above-mentioned compounds, medicaments containing them and their manufacture, as well as the use of the above-mentioned compounds in the control or prevention of illnesses such as cancer.Type: ApplicationFiled: June 23, 2008Publication date: July 1, 2010Inventors: Guy Georges, Eike Hoffmann, Klaus Kaluza, Matthias Koerner, Ulrike Reiff, Stefan Weigand
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Patent number: 7745467Abstract: The invention concerns compounds of general formula (I), wherein n, X1, X2, X3, X4, Y and W are as defined herein. The invention also concerns a method for preparing said compounds and their therapeutic use.Type: GrantFiled: January 8, 2008Date of Patent: June 29, 2010Assignee: Sanofi-AventisInventors: Laurent Dubois, Yannick Evanno, Andre Malanda
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Publication number: 20100160381Abstract: The invention relates to the use of an Raf inhibitor for the manufacture of pharmaceutical compositions for the treatment of thyroid cancer, more specifically papillary thyroid cancer (PTC); the use of a Raf inhibitor in the treatment of thyroid cancer, more specifically PTC; a method of treating warm-blooded animals including mammals, especially humans, suffering from thyroid cancer, more specifically PTC, by administering to a said animal in need of such treatment a dose effective against said disease of an Raf inhibitor. The invention also relates to the use of a Raf inhibitor in combination with a platin compound for the treatment of thyroid cancer, more specifically papillary thyroid cancer.Type: ApplicationFiled: May 21, 2008Publication date: June 24, 2010Applicant: Novartis AGInventor: Darrin Douglas Stuart
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Publication number: 20100152183Abstract: Disclosed are compounds which inhibit the activity of anti-apoptotic Bcl-2 or Bcl-xL proteins, compositions containing the compounds and methods of treating diseases during which are expressed anti-apoptotic Bcl-2 protein.Type: ApplicationFiled: December 4, 2009Publication date: June 17, 2010Applicant: ABBOTT LABORATORIESInventors: Milan Bruncko, Hong Ding, George A. Doherty, Steven W. Elmore, Lisa Hasvold, Laura Hexamer, Aaron Kunzer, Robert A. Mantei, William J. McClellan, Chang H. Park, Cheol-Min Park, Andrew M. Petros, Xiaohong Song, Andrew J. Souers, Gerard M. Sullivan, Zhi-Fu Tao, Gary T. Wang, Le Wang, Xilu Wang, Michael D. Wendt