Additional Hetero Ring Attached Directly Or Indirectly To The Diazole Ring By Nonionic Bonding (e.g., Methyl( 5-[2-(2-thienyl)-1,3-dioxolan -2-yl]-1h-benzimidazol-2-yl) Carbamate, Etc.) Patents (Class 548/304.7)
  • Patent number: 10569189
    Abstract: A process for producing THC-O-acetate using a succession of distillation, salting-out assisted liquid-liquid extractions (SALLEs), and solvent recovery techniques. Tetrahydrocannabinol (THC) in cannabis oil reacts with acetic anhydride under reflux to produce THC-O-acetate and acetic acid. The resulting crude product is distilled and subjected to a SALLE with hexane followed by a SALLE with petroleum ether, before being distilled again in order to obtain a refined, THC-O-acetate product.
    Type: Grant
    Filed: May 17, 2019
    Date of Patent: February 25, 2020
    Assignee: Nextleaf Solutions Ltd.
    Inventors: Krupal Devendra Pal, Ryan Delmoral Ko, Brock Aston Hughes, Ivan Jason Casselman
  • Patent number: 9675595
    Abstract: A pharmaceutical combination comprising (a) the phosphatidylinositol 3-kinase (PI3K) inhibitor compound (S)-pyrrolidine-1,2-dicarboxylic acid 2-amide 1-({4-methyl-5-[2-(2,2,2-trifluoro-1,1-dimethyl-ethyl)-pyridin-4-yl]thiazol-2-yl}-amide) or a pharmaceutically acceptable salt thereof, and (b) at least one mitogen activated protein kinase (MEK) inhibitor or a pharmaceutically acceptable salt, and optionally at least one pharmaceutically acceptable carrier, for simultaneous, separate or sequential administration; the uses of such combination in the treatment of proliferative diseases; and methods of treating a subject suffering from a proliferative disease comprising administering a therapeutically effective amount of such combination.
    Type: Grant
    Filed: August 30, 2012
    Date of Patent: June 13, 2017
    Assignee: Novartis AG
    Inventors: Christine Fritsch, Xizhong Huang, Markus Boehm, Emmanuelle di Tomaso, Jan Cosaert
  • Patent number: 9156796
    Abstract: The present invention relates to benzoimidazole-carboxylic acid amide compounds of the formula I, in which R?, R?, R??, R1, R2, R3, R4, R5, R6 and Z are defined as indicated below. The compounds of the formula I are APJ receptor modulators, and are useful for the treatment of diseases associated with increased blood pressure for example. The invention furthermore relates to the use of compounds of the formula I, in particular as active ingredients in pharmaceuticals, and pharmaceutical compositions comprising them.
    Type: Grant
    Filed: September 19, 2013
    Date of Patent: October 13, 2015
    Assignee: SANOFI
    Inventors: Stephanie Hachtel, Paulus Wohlfart, John Weston, Marco Mueller, Elisabeth Defossa, Katharina Mertsch, Jian-Hui Weng, Robert Alan Binnie, Farid Abdul-Latif, William Jerome Bock, Armin Walser
  • Patent number: 9126975
    Abstract: The present invention relates to a process for the preparation of statins by means of a Julia-Kocienski reaction between an aldehyde and a sulfone derivative in the presence of an alkaline metal alkoxy base. The resulting derivatives are suitable as building blocks for statin type compounds such as cerivastatin, fluvastatin, pitavastatin and rosuvastatin.
    Type: Grant
    Filed: January 13, 2012
    Date of Patent: September 8, 2015
    Assignee: DSM SINOCHEM PHARMACEUTICALS NETHERLANDS B.V.
    Inventors: Karin Henderika Maria Bessembinder, Dennis Heemskerk, Ben De Lange
  • Publication number: 20150133500
    Abstract: The invention provides compounds that are useful as sodium channel blockers. In one aspect, the invention provides compounds of Formula I: and pharmaceutically acceptable salts, solvates, hydrates, or diastereomers thereof, wherein W1, W2, W3, W4, U, G, m, R1, and R2 are defined in the disclosure. In certain embodiments, the invention provides compounds of Formulae II to V as set forth supra. The invention also provides the use of compounds of any of the above discussed formulae to treat a disorder responsive to blockade of sodium channels. In one embodiment, Compounds of the Invention are useful for treating pain.
    Type: Application
    Filed: November 6, 2014
    Publication date: May 14, 2015
    Inventors: Laykea Tafesse, Jiangchao Yao, Xiaoming Zhou
  • Patent number: 9024040
    Abstract: Provided are processes for the preparation of benzimidazole structures having Formula VIIIb-1: and salts and solvates thereof, wherein Z, X5, R2b, R2c and R10 are as defined herein. Compounds of Formula VIIIb-1 are useful for the preparation of benzimidazole derivatives.
    Type: Grant
    Filed: September 13, 2012
    Date of Patent: May 5, 2015
    Assignee: Array Biopharma Inc.
    Inventors: John DeMattei, Sagar Shakya, Anthony D. Piscopio, Bruno P. Hache, Matthew Charles Evans, James Gair Ford, Simon Mark Pointon, Koen Peeters, Timothy John Lilley, John Leonard
  • Publication number: 20150119436
    Abstract: The invention relates to the compounds of formula I and formula II or its pharmaceutical acceptable salts, as well as polymorphs, solvates, enantiomers, stereoisomers and hydrates thereof. The pharmaceutical compositions comprising an effective amount of compounds of formula I or formula II; and methods for treating or preventing blood clotting disorders may be formulated for oral, buccal, rectal, topical, transdermal, transmucosal, intravenous, parenteral administration, syrup, or injection. Such compositions may be used to treatment of strokes in those with atrial fibrillation due to causes other than heart valve disease, and at least one additional risk factor for stroke (congestive heart failure, hypertension, age, diabetes, and prior stroke), and to prevent the formation of blood clots in the veins in adults operated to replace a hip or knee.
    Type: Application
    Filed: March 24, 2013
    Publication date: April 30, 2015
    Inventor: Mahesh Kandula
  • Patent number: 8980920
    Abstract: The present invention relates to novel Linked Tricyclic Aryl Compounds, compositions comprising at least one Linked Tricyclic Compound, and methods of using Linked Tricyclic Aryl Compounds for treating or preventing HCV infection in a patient. in one aspect, the present invention provides Compounds of Formula (I): and pharmaceutically acceptable salts thereof, wherein: Non-limiting examples of the Compounds of Formula (II) include compound 56.
    Type: Grant
    Filed: May 28, 2010
    Date of Patent: March 17, 2015
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Qingbei Zeng, Kevin X. Chen, Anilkumar Gopinadhan Nair, Stuart B. Rosenblum, Joseph A. Kozlowski, F. George Njoroge
  • Publication number: 20150011774
    Abstract: The present invention relates to a process for the preparation of azilsartan medoxomil or pharmaceutically acceptable salts thereof.
    Type: Application
    Filed: January 30, 2013
    Publication date: January 8, 2015
    Inventors: Md Abul Kalam Azad, Prakash Bhimaji Kshirsagar, Shravan Kumar Singh, Anand Prakash Tiwari, Kaptan Singh, Mohan Prasad, Sudershan Kumar Arora
  • Publication number: 20140378421
    Abstract: The present invention relates to novel compounds having ?2 adrenergic agonist and M3 muscarinic antagonist dual activity, to pharmaceutical compositions containing them, to the process for their preparation and to their use in respiratory therapies.
    Type: Application
    Filed: November 9, 2012
    Publication date: December 25, 2014
    Inventors: Jose Aiguade Bosch, Silvia Gual Roig, Maria Prat Quinones, Carlos Puig Duran
  • Patent number: 8901313
    Abstract: The invention relates to novel compounds of Formula I: wherein A, Y, R1, R2 and the subscript b each has the meaning as described herein and compounds of Formula I, and stereoisomers, geometric isomers, tautomers, solvates, metabolites, isotopes, pharmaceutically acceptable salts, or prodrugs thereof. Compounds of Formula I and pharmaceutical compositions thereof are useful in the treatment of disease and disorders in which undesired or over-activation of NF-kB signaling is observed.
    Type: Grant
    Filed: March 15, 2012
    Date of Patent: December 2, 2014
    Assignee: Genentech, Inc.
    Inventors: Steven Staben, Jianwen Feng, Pui Leng Loke, Christian A. G. N. Montalbetti
  • Patent number: 8895756
    Abstract: The present invention provides pharmaceutical formulations of lyophilized bendamustine suitable for pharmaceutical use. The present invention further provides methods of producing lyophilized bendamustine. The pharmaceutical formulations can be used for any disease that is sensitive to treatment with bendamustine, such as neoplastic diseases.
    Type: Grant
    Filed: December 19, 2012
    Date of Patent: November 25, 2014
    Assignee: Cephalon, Inc.
    Inventors: Jason Edward Brittain, Joe Craig Franklin
  • Publication number: 20140343049
    Abstract: The present invention relates to compounds of formula (IA) wherein QA is QA1 or QA2 P is P1, heterocycyl or heterocyclyl substituted by one to five Z; and wherein A1, A2, A3, A4, G1, Z, R1, R2, R3 and R4 are as defined in claim 1; or a salt or N-oxide thereof. Furthermore, the present invention relates to processes and intermediates for preparing compounds of formula (IA), to insecticidal, acaricidal, nematicidal and molluscicidal compositions comprising the compounds of formula (IA) and to methods of using the compounds of formula (IA) to control insect, acarine, nematode and mollusc pests.
    Type: Application
    Filed: August 10, 2012
    Publication date: November 20, 2014
    Applicant: SYNGENTA PARTICIPATIONS AG
    Inventors: Julie Clementine Toueg, Tomas Smejkal, Sebastian Volker Wendeborn, Jerome Yves Cassayre, Myriem El Qacemi, Bernhard Breit, Lisa Diab, Regis Jean Georges Mondiere, Nicolas Poirier
  • Publication number: 20140302010
    Abstract: The present invention relates to substituted benzimidazole compounds of general formula (I) in which R3, R5 and A are as defined in the claims, to methods of preparing said compounds, to pharmaceutical compositions and combinations comprising said compounds and to the use of said compounds for manufacturing a pharmaceutical composition for the treatment or prophylaxis of a disease, in particular of a hyper-proliferative and/or angiogenesis disorder, as a sole agent or in combination with other active ingredients.
    Type: Application
    Filed: March 28, 2012
    Publication date: October 9, 2014
    Applicant: BAYER INTELLECTUAL PROPERTY GMBH
    Inventors: Ulrich Klar, Marcus Koppitz, Duy Nguyen, Dirk Kosemund, Roland Neuhaus, Gerhard Siemeister
  • Publication number: 20140303127
    Abstract: The present invention relates to novel compounds having ?2 adrenergic agonist and M3 muscarinic antagonist dual activity, to pharmaceutical compositions containing them, to the process for their preparation and to their use in respiratory therapies.
    Type: Application
    Filed: November 9, 2012
    Publication date: October 9, 2014
    Inventors: Jose Aiguade Bosch, Silvia Gual Roig, Maria Prat Quinones, Carlos Puig Duran
  • Patent number: 8835647
    Abstract: 2-((R)-2-Methylpyrrolidin-2-yl)-1H-benzimidazole-4-carboxamide Crystalline Form 1, ways to make it, compositions comprising it and made using it, and methods of treating patients having disease using it are disclosed.
    Type: Grant
    Filed: September 27, 2013
    Date of Patent: September 16, 2014
    Assignee: AbbVie Inc.
    Inventor: Lawrence Kolaczkowski
  • Publication number: 20140249196
    Abstract: The invention provides molecular entities that bind with high affinity to PPARG (PPAR?), inhibit cdk5-mediated phosphorylation of PPARG, but do not exert an agonistic effect on PPARG. Compounds of the invention can be used for treatment of conditions in patients wherein PPARG plays a role, such as diabetes or obesity. Methods of preparation of the compounds, bioassay methods for evaluating compounds of the invention as non-agonistic PPARG binding compounds, and pharmaceutical compositions are also provided.
    Type: Application
    Filed: November 20, 2012
    Publication date: September 4, 2014
    Inventors: Theodore Mark Kamenecka, Patrick R. Griffin, Amy S. Ripka, Jeffrey O. Saunders
  • Publication number: 20140243331
    Abstract: This invention describes the development of targeted small molecule inhibitors of the inv(16) fusion, the causative agent in ˜12% of acute myeloid leukemia (AML). The inv(16) fusion results in expression of the CBF?-SMMHC fusion protein in the blood cells of afflicted patients. The present invention provides compounds which inhibit the function of both CBF? and the CBF?-SMMHC fusion. These compounds block the growth of an inv(16) leukemia cell line as well as increase its apoptosis, while showing minimal effects against non inv(16) cell lines. As a mechanism to develop inhibitors with selectivity for the CBF?-SMMHC fusion protein, the present invention further provides dimeric derivatives of these compounds which show both increased potency as well as selectivity for CBF?-SMMHC. These compounds show potent inhibition of an inv(16) leukemia cell line with minimal effects on non inv(16) cell lines.
    Type: Application
    Filed: May 7, 2014
    Publication date: August 28, 2014
    Applicant: UNIVERSITY OF VIRGINIA PATENT FOUNDATION
    Inventors: John H. Bushweller, Jolanta Grembecka, Anuradha Illendula, Lauren Dixon
  • Publication number: 20140243308
    Abstract: The present invention relates to substituted imidazopyridazines and substituted benzimidazoles, as well as pharmaceutical compositions comprising the same, which are FGFR3 inhibitors useful in the treatment of cancer and other diseases.
    Type: Application
    Filed: May 1, 2014
    Publication date: August 28, 2014
    Applicant: Incyte Corporation
    Inventors: Wenqing Yao, Colin Zhang, Meizhong Xu, Jincong Zhuo, Chunhong He
  • Patent number: 8802865
    Abstract: The present invention is directed to a novel 2-substituted benzimidazole derivatives, pharmaceutical compositions containing them and their use in the treatment of disorders and conditions modulated by the androgen receptor.
    Type: Grant
    Filed: October 1, 2013
    Date of Patent: August 12, 2014
    Assignee: Janssen Pharmaceutica, NV
    Inventors: Vernon C Alford, Jr., James C Lanter, Raymond A Ng
  • Publication number: 20140221339
    Abstract: The present invention provides a novel heterocyclic derivative or a pharmaceutically acceptable salt thereof. For example, the present invention provides a heterocyclic derivative of the general formula [1] or its tautomer, or a pharmaceutically acceptable salt thereof: wherein R1 and R2 are the same or different aromatic rings, etc., and ring A is a heterocyclic ring. The compound of the invention or a pharmaceutically acceptable salt thereof has potent mPGES-1 inhibiting activity and is useful as an agent for the treatment or prevention of a disease, such as rheumatoid arthritis, osteoarthritis, temporomandibular joint disorders, low back pain, endometriosis, dysmenorrhea, overactive bladder, malignant tumors or neurodegenerative disease.
    Type: Application
    Filed: August 17, 2012
    Publication date: August 7, 2014
    Applicant: NIPPON SHINYAKU CO., LTD.
    Inventor: Hironori Otsu
  • Publication number: 20140221431
    Abstract: Disclosed in the present invention is a novel histone deacetylase inhibitor of benzamides and use thereof. The inhibitor has good efficacy in treating diseases caused by abnormal gene expression, such as tumours, endocrine disorders, immune system diseases, genetic diseases and nerve system diseases. The histone deacetylase inhibitor of benzamides is a compound of the following general chemical structural formula (I) or a salt thereof.
    Type: Application
    Filed: June 26, 2012
    Publication date: August 7, 2014
    Applicants: Shanghai Institute of Pharmaceutical Industry, Sinopharm A-think Pharmaceutical Co., Ltd
    Inventors: Jianqi Li, Qingwei Zhang, Zhidan Jia, Jiajing Wang
  • Patent number: 8791270
    Abstract: The present invention provides pharmaceutical formulations of lyophilized bendamustine suitable for pharmaceutical use. The present invention further provides methods of producing lyophilized bendamustine. The pharmaceutical formulations can be used for any disease that is sensitive to treatment with bendamustine, such as neoplastic diseases.
    Type: Grant
    Filed: August 19, 2013
    Date of Patent: July 29, 2014
    Assignee: Cephalon, Inc.
    Inventors: Jason Edward Brittain, Joe Craig Franklin
  • Patent number: 8772505
    Abstract: The present invention relates to novel Tricyclic Compounds, compositions comprising at least one Tricyclic Compound, and methods of using Tricyclic Compounds for treating or preventing a viral infection or a virus-related disorder in a patient. The present invention provides Tricyclic Compounds of Formula (I): Non-limiting examples of the Compounds of Formula (I) include compound 44 The Compounds of Formula (II) can be useful for inhibiting HCV viral replication or replicon activity, and for treating or preventing HCV infection in a patient.
    Type: Grant
    Filed: May 28, 2010
    Date of Patent: July 8, 2014
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Kevin X. Chen, Anilkumar Gopinadhan Nair, Qingbei Zeng, Stuart B. Rosenblum, Joseph A. Kozlowski, F. George Njoroge
  • Patent number: 8759520
    Abstract: Compounds of general formula (I): wherein R1, R2, R3, R4, R5, R6, X and Y are as defined herein are inhibitors of Bcl-2 and are useful for treating diseases characterized by abnormal cell growth and/or dysregulated apoptosis.
    Type: Grant
    Filed: December 8, 2009
    Date of Patent: June 24, 2014
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Stephen Peter East, Mark Whittaker, Osamu Ichihara, Adrian Kotei Kotey, Smantha Jayne Bamford
  • Publication number: 20140171363
    Abstract: The present invention provides compounds of formula (I); or pharmaceutically acceptable salts thereof, wherein the variables are defined as herein. The present invention provides a method for manufacturing the compounds of formula (I), their therapeutic uses, combinations with other of pharmacologically active agents, and a pharmaceutical compositions.
    Type: Application
    Filed: February 24, 2014
    Publication date: June 19, 2014
    Applicant: NOVARTIS AG
    Inventors: David Weninger BARNES, Gregory Raymond BEBERNITZ, Kevin CLAIRMONT, Scott Louis COHEN, Robert Edson DAMON, II, Robert Francis DAY, Stephanie Kay DODD, Christoph GAUL, Hatice Belgin GULGEZE EFTHYMIOU, Monish JAIN, Rajeshri Ganesh KARKI, Louise Clare KIRMAN, Kai LIN, Justin Yik Ching MAO, Tajesh Jayprakash PATEL, Brian Kenneth RAYMER, SU Liansheng
  • Patent number: 8691998
    Abstract: Novel N-heterocyclic carbene ligand precursors, N-heterocyclic carbene ligands and N-heterocyclic metal-carbene complexes are provided. Metal-carbene complexes comprising N-heterocyclic carbene ligands can be chiral, which are useful for catalyzing enantioselective synthesis. Methods for the preparation of the N-heterocyclic carbene ligands and N-heterocyclic metal-carbene complexes are given.
    Type: Grant
    Filed: March 8, 2013
    Date of Patent: April 8, 2014
    Assignee: University of Florida Research Foundation, Inc.
    Inventors: Adam S. Veige, Mathew S. Jeletic, Roxy J. Lowry, Khalil A. Abboud
  • Publication number: 20140094450
    Abstract: The present invention relates to benzoimidazole-carboxylic acid amide compounds of the formula I, in which R?, R?, R??, R1, R2, R3, R4, R5, R6 and Z are defined as indicated below. The compounds of the formula I are APJ receptor modulators, and are useful for the treatment of diseases associated with increased blood pressure for example. The invention furthermore relates to the use of compounds of the formula I, in particular as active ingredients in pharmaceuticals, and pharmaceutical compositions comprising them.
    Type: Application
    Filed: September 19, 2013
    Publication date: April 3, 2014
    Applicant: SANOFI
    Inventors: Stephanie HACHTEL, Paulus WOHLFART, John WESTON, Marco MUELLER, Elisabeth DEFOSSA, Katharina MERTSCH, Jian-Hui WENG, Robert Alan BINNIE, Farid ABDUL-LATIF, William Jerome BOCK, Armin WALSER
  • Patent number: 8658207
    Abstract: The present invention provides pharmaceutical release systems comprising an therapeutically effective amount of flibanserin and at least one pharmaceutically acceptable excipient, characterized in that said pharmaceutical release systems exhibit a pharmacokinetic profile that is characterized by an average maximum flibanserin plasma concentration Cmax lower than 300 ng/mL, preferably lower than 200 ng/mL after administration of a single dose to healthy volunteers in fasted state or directly after a meal.
    Type: Grant
    Filed: August 13, 2007
    Date of Patent: February 25, 2014
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Wolfram Eisenreich, Thomas Friedl, Florian Sommer, Nantharat Pearnchob, Karl G. Wagner
  • Patent number: 8653259
    Abstract: The invention provides the process illustrated in scheme 1 for synthesizing heterocyclic compounds of formula I. In the process, an isothiocyanate of formula II is initially reacted with a primary amine or formula III to give a thiourea of formula IV. Subsequently, the thiourea of formula IV is converted to the corresponding heterocycle of formula I using a base and a sulfonyl chloride.
    Type: Grant
    Filed: February 6, 2008
    Date of Patent: February 18, 2014
    Assignee: Sanofi-Aventis Deutschland GmbH
    Inventors: Uwe Heinelt, Hans-Jochen Lang
  • Publication number: 20140031317
    Abstract: The present invention is directed to a novel 2-substituted benzimidazole derivatives, pharmaceutical compositions containing them and their use in the treatment of disorders and conditions modulated by the androgen receptor.
    Type: Application
    Filed: October 1, 2013
    Publication date: January 30, 2014
    Applicant: Janssen Pharmaceutica, NV
    Inventors: Vernon C Alford, JR., James C. Lanter, Raymond A. Ng
  • Patent number: 8609863
    Abstract: The present invention provides pharmaceutical formulations of lyophilized bendamustine suitable for pharmaceutical use. The present invention further provides methods of producing lyophilized bendamustine. The pharmaceutical formulations can be used for any disease that is sensitive to treatment with bendamustine, such as neoplastic diseases.
    Type: Grant
    Filed: December 19, 2012
    Date of Patent: December 17, 2013
    Assignee: Cephalon, Inc.
    Inventors: Jason Edward Brittain, Joe Craig Franklin
  • Publication number: 20130324529
    Abstract: 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: Application
    Filed: August 6, 2013
    Publication date: December 5, 2013
    Applicant: JANSSEN PHARMACEUTICA NV
    Inventors: Henricus Jacobus Maria Gijsen, Michel Anna Jozef De Cleyn, Michel Surkyn, Bie Maria Pieter Verbist
  • Patent number: 8598078
    Abstract: Compounds of Formula I wherein the substituents are as defined in Claim 1, and the agrochemically acceptable salts and all stereoisomers and tautomeric forms of the compounds of formula I can be used as agrochemical active ingredients and can be prepared in a manner known per se.
    Type: Grant
    Filed: August 21, 2008
    Date of Patent: December 3, 2013
    Assignee: Syngenta Crop Protection, LLC
    Inventors: Olivier Loiseleur, Roger Graham Hall, André Denis Stoller, Gerald Wayne Craig, André Jeanguenat, Andrew Edmunds
  • Publication number: 20130303571
    Abstract: 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: Application
    Filed: July 15, 2013
    Publication date: November 14, 2013
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: Roland PFAU, Kirsten ARNDT, Henri DOODS, Klaus KLINDER, Raimund KUELZER, Dimitrijs LUBRIKS, Juergen MACK, Benjamin PELCMAN, Henning PRIEPKE, Robert ROENN, Dirk STENKAMP, Edgars SUNA
  • Publication number: 20130281392
    Abstract: The invention relates to oral, topical or injectable compositions for combating liver fluke parasites in mammals, comprising at least one benzimidazole derivative active agent. The invention also provides for an improved method for eradicating and controlling liver fluke parasite infections and infestations in a mammal comprising administering the compositions of the invention to the mammal in need thereof.
    Type: Application
    Filed: April 18, 2013
    Publication date: October 24, 2013
    Applicant: MERIAL LIMITED
    Inventor: Charles Q. Meng
  • Publication number: 20130267711
    Abstract: The invention provides a method of activating PPAR ? and a method of treating or preventing a disease associated with PPAR ? by administering a tricyclic compound having a PPAR ? agonist activity, which is represented by the formula (I) wherein Z represents a single bond or the like, Y represents a hydrogen atom, lower alkyl optionally having substituent(s) or the like, X represents a hydrogen atom or the like, A represents aryl or the like, B and C are the same or different and each represents an aromatic carbocycle or the like, R4-R9 are the same or different and each represents hydrogen or the like, V represents a single bond or the like, R10 and R11 are the same or different and each represents hydrogen or the like, or a pharmaceutically acceptable salt thereof or the like:
    Type: Application
    Filed: June 3, 2013
    Publication date: October 10, 2013
    Inventors: Arata YANAGISAWA, Keiji UEHARA, Masahiro MATSUBARA, Kimihisa UENO, Michihiko SUZUKI, Takeshi KUBOYAMA, Keisuke YAMAMOTO, Tomohiro TAMURA
  • Patent number: 8545886
    Abstract: The invention is directed to a Pharmaceutical extended release system, particularly for oral administration, of a pH-dependent water-soluble active substance, comprising or essentially consisting of a) flibanserin or a pharmaceutically acceptable derivative thereof as active substance; b) one or more pharmaceutically acceptable pH-dependent polymers; c) one or more pharmaceutically acceptable pH-independent polymers; d) one or more pharmaceutically acceptable acids; and e) optionally one or more additives. The present invention provides a release profile of flibanserin which is independent on the pH in the gastrointestinal tract when administered orally resulting in a significantly improved bioavailability.
    Type: Grant
    Filed: August 13, 2007
    Date of Patent: October 1, 2013
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Wolfram Eisenreich, Thomas Friedl
  • Publication number: 20130231344
    Abstract: Described herein are compounds and pharmaceutical compositions containing such compounds, which modulate the activity of store-operated calcium (SOC) channels. Also described herein are methods of using such SOC channel modulators, alone and in combination with other compounds, for treating diseases or conditions that would benefit from inhibition of SOC channel activity.
    Type: Application
    Filed: January 4, 2013
    Publication date: September 5, 2013
    Applicant: CalciMedica, Inc.
    Inventors: Gonul Velicelebi, Kenneth A. Stauderman, Jeffrey P. Whitten, Yazhong Pei, Jianguo Cao, Zhijun Wang, Evan Rogers, Brian Dyck, Jonathan Grey
  • Patent number: 8524914
    Abstract: The present invention relates to novel intermediate compounds used in preparing Rosuvastatin or the pharmaceutically acceptable salts thereof, to a method for preparing same, and to a method for preparing Rosuvastatin or the pharmaceutically acceptable salts thereof from the intermediates. The preparation method of the present invention has the effect of providing Rosuvastatin hemi-calcium salts with an excellent yield rate.
    Type: Grant
    Filed: April 8, 2010
    Date of Patent: September 3, 2013
    Assignee: Chong Kun Dang Pharmaceutical Corp.
    Inventors: Hongwoo Lee, Daejong Park, Choongleol Yoo, Donghyuk Nam, Hohyung Ryu, Dongjin Kim
  • Patent number: 8513293
    Abstract: Disclosed are methods for inhibiting abnormal cell growth or treating hyperproliferative diseases in mammals, comprising administering to a mammal in heed thereof a pharmaceutical composition comprising 6-(4-bromo-2-fluorophenylamino)-7-fluoro-3-methyl-3H-benzoimidazole-5-carboxylic acid (2-hydroxy-ethoxy)-amide, or a pharmaceutically acceptable salt thereof, in combination with an effective amount of an anti-tumor agent or in combination with radiation therapy.
    Type: Grant
    Filed: May 3, 2012
    Date of Patent: August 20, 2013
    Assignee: Array BioPharma Inc.
    Inventors: Eli M. Wallace, Joseph P. Lyssikatos, Allison L. Marlow, T. Brian Hurley
  • Publication number: 20130210024
    Abstract: The present technology relates to a method of treating cancer by sensitizing human tumours to DNA damaging therapies through activating FBXO32 expression. Transactivation of FBXO32 through the inhibition of EZH2, a histone methyltransferase, decreases p21 protein induction which results in the sensitization of human tumours to chemotherapy. The method further provides a prognostic method to determine if a combination treatment would be effective.
    Type: Application
    Filed: October 14, 2011
    Publication date: August 15, 2013
    Applicant: Agency for Science, Technology and Research
    Inventors: Qiang Yu, Zhenlong Wu
  • Patent number: 8501956
    Abstract: Provided are compounds having Formula VIIIa-1: wherein Z, X5, R2, R2a and R10 are as defined herein. Compounds of Formula VIIIa-1 can be used to prepare heterocyclic derivatives such as benzimidazole derivatives.
    Type: Grant
    Filed: September 9, 2011
    Date of Patent: August 6, 2013
    Assignees: Array BioPharma Inc., AstraZeneca SB
    Inventors: John Demattei, Sagar Shakya, Anthony D. Piscopio, Bruno P. Hache, Matthew Charles Evans, James Gair Ford, Simon Mark Pointon, Koen Peeters, Timothy John Lilley, John Leonard
  • Patent number: 8501957
    Abstract: 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: Grant
    Filed: December 10, 2009
    Date of Patent: August 6, 2013
    Assignee: China Medical University
    Inventors: Chih-Shiang Chang, Jih-Hwa Guh, Che-Ming Teng, Shiow-Lin Pan, Wei-Ling Chang, Ju-Fang Liu, Kai-Wei Chang, Sheng-Chu Kuo
  • Patent number: 8471038
    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: Grant
    Filed: December 25, 2009
    Date of Patent: June 25, 2013
    Assignee: Dainippon Sumitomo Pharma Co., Ltd.
    Inventors: Katsunori Tsuboi, Yusuke Yamai, Hitoshi Watanabe, Hironori Kinoshita
  • Patent number: 8461350
    Abstract: The present invention provides pharmaceutical formulations of lyophilized bendamustine suitable for pharmaceutical use. The present invention further provides methods of producing lyophilized bendamustine. The pharmaceutical formulations can be used for any disease that is sensitive to treatment with bendamustine, such as neoplastic diseases.
    Type: Grant
    Filed: October 18, 2012
    Date of Patent: June 11, 2013
    Assignee: Cephalon, Inc.
    Inventors: Jason Edward Brittain, Joe Craig Franklin
  • Patent number: 8461351
    Abstract: A sterically bulky stabilizer that includes an alkylated-benzimidazolone compound, where the sterically bulky stabilizer is associated non-covalently with a benzimidazolone pigment, and the presence of the sterically bulky stabilizer limits the extent of particle growth and aggregation, to afford nanoscale pigment particles.
    Type: Grant
    Filed: July 28, 2011
    Date of Patent: June 11, 2013
    Assignees: Xerox Corporation, National Research Council of Canada
    Inventors: Rina Carlini, Darren Andrew Makeiff
  • Publication number: 20130143841
    Abstract: Embodiments herein provide compounds and methods of making and using such compounds for prevention and treatment of multidrug resistant bacteria. In particular, embodiments are directed to anti-bacterial agents from benzo[d]heterocyclic scaffolds for prevention and treatment of multidrug resistant bacteria.
    Type: Application
    Filed: January 29, 2013
    Publication date: June 6, 2013
    Applicant: UNIVERSITY OF NOTRE DAME DU LAC
    Inventor: UNIVERSITY OF NOTRE DAME DU LAC
  • Patent number: 8455661
    Abstract: Novel N-heterocyclic carbene ligand precursors, N-heterocyclic carbene ligands and N-heterocyclic metal-carbene complexes are provided. Metal-carbene complexes comprising N-heterocyclic carbene ligands can be chiral, which are useful for catalyzing enantioselective synthesis. Methods for the preparation of the N-heterocyclic carbene ligands and N-heterocyclic metal-carbene complexes are given.
    Type: Grant
    Filed: February 15, 2008
    Date of Patent: June 4, 2013
    Assignee: University of Florida Research Foundation, Inc.
    Inventors: Adam Steven Veige, Mathew S. Jeletic, Roxy J. Lowry, Khalil A. Abboud
  • Patent number: 8450498
    Abstract: Ionic liquid epoxide monomers capable of reacting with cross-linking agents to form polymers with high tensile and adhesive strengths. Ionic liquid epoxide monomers comprising at least one bis(glycidyl) N-substituted nitrogen heterocyclic cation are made from nitrogen heterocycles corresponding to the bis(glycidyl) N-substituted nitrogen heterocyclic cations by a method involving a non-nucleophilic anion, an alkali metal cation, epichlorohydrin, and a strong base.
    Type: Grant
    Filed: May 14, 2011
    Date of Patent: May 28, 2013
    Assignee: AZ Technology, Inc.
    Inventor: Mark S. Paley