1,3-diazoles (including Hydrogenated) Patents (Class 548/300.1)
  • Patent number: 10383832
    Abstract: The present invention relates to modified release pharmaceutical composition comprising metoprolol succinate, one or more release modifying agent(s) and one or more pharmaceutically acceptable excipient(s). More specifically, the invention relates to modified release pharmaceutical compositions comprising metoprolol succinate and a process for preparation thereof.
    Type: Grant
    Filed: December 24, 2016
    Date of Patent: August 20, 2019
    Inventor: Laxminarayan Joshi
  • Patent number: 9801858
    Abstract: An object of the present invention is to provide a pharmaceutical agent which is administered to a patient with chronic kidney disease in which the progress of worsening of renal function is rapid whereby the progress of the symptom is suppressed or improved. The present invention relates to a progress-suppressing or improving agent for chronic kidney disease containing 5-hydroxy-1-methylhydantoin as an active ingredient. The pharmaceutical agent of the present invention showed a significant effect in a patient with chronic kidney disease where progress of the renal function decrease is rapid. The present pharmaceutical agent is very useful as a highly safe pharmaceutical agent which suppresses or improves the progress of worsening of the renal function of a patient with rapidly progressive chronic kidney disease for which there has been no effective therapeutic agent being simply and easily ingestible.
    Type: Grant
    Filed: February 25, 2015
    Date of Patent: October 31, 2017
    Assignee: NIPPON ZOKI PHARMACEUTICAL CO., LTD.
    Inventor: Kazuharu Ienaga
  • Patent number: 9018390
    Abstract: The present disclosure relates to compounds, compositions and methods for the treatment of hepatitis C virus (HCV) infection. Also disclosed are pharmaceutical compositions containing such compounds and methods for using these compounds in the treatment of HCV infection.
    Type: Grant
    Filed: June 17, 2013
    Date of Patent: April 28, 2015
    Assignee: Bristol-Myers Squibb Company
    Inventors: Carol Bachand, Makonen Belema, Daniel H. Deon, Andrew C. Good, Jason Goodrich, Clint A. James, Rico Lavoie, Omar D. Lopez, Alain Martel, Nicholas A. Meanwell, Van N. Nguyen, Jeffrey Lee Romine, Edward H. Ruediger, Lawrence B. Snyder, Denis R. St. Laurent, Fukang Yang, David R. Langley, Lawrence G. Hamann
  • Publication number: 20150099800
    Abstract: The invention provides for novel lipase inhibitors, and compositions and devices comprising the same. The invention further provides for methods for treatment of disorders comprising administration of novel diacylglycerol lipase inhibitors, and compositions and devices comprising said inhibitors. In some embodiments, the disorders are pancreatitis, obesity, shock or pancreatic necrosis. The invention further provides for novel ether lipid reporter compounds and methods of assaying enzymatic activity comprising contacting a compound with a novel ether lipid reporter compound.
    Type: Application
    Filed: May 24, 2013
    Publication date: April 9, 2015
    Inventor: Richard I. Duclos, JR.
  • Patent number: 8981119
    Abstract: The present invention is directed to compounds of Formula I: wherein R1, R2, R3, R4, R5, X and n are described herein. These compounds and their pharmaceutically acceptable salts thereof are useful as IK1 channel activators.
    Type: Grant
    Filed: June 6, 2014
    Date of Patent: March 17, 2015
    Assignee: Astellas Pharma Inc.
    Inventors: Tsukasa Ishihara, Kazuhiro Ikegai, Ikumi Kuriwaki, Hiroyuki Hisamichi, Nobuaki Takeshita, Ryuichi Takezawa
  • Patent number: 8933242
    Abstract: This disclosure relates to new metal complexes, such as compounds of Formula 1, and their application in olefin or alkyne metathesis and to methods of carrying out olefin metathesis reactions.
    Type: Grant
    Filed: June 18, 2013
    Date of Patent: January 13, 2015
    Assignee: Apeiron Synthesis S.A.
    Inventors: Krzysztof Skowerski, Michal Bieniek
  • Publication number: 20150004322
    Abstract: N-heterocyclic (“NHC”) carbenes and NHC carbene-metal complexes. The NHC carbene having a formula: wherein R1 is an aromatic or aliphatic group, and R2 is an aromatic or aliphatic group, R3 is a fluorinated alkyl chain, R4 is a fluorinated alkyl chain or a proton.
    Type: Application
    Filed: June 26, 2013
    Publication date: January 1, 2015
    Inventor: Rusty Lew Blanski
  • Patent number: 8921340
    Abstract: The present invention features the use of a synthetic triterpenoid to induce gene expression and differentiation of stem or progenitor cells in the treatment of bone/cartilage diseases or conditions.
    Type: Grant
    Filed: May 8, 2012
    Date of Patent: December 30, 2014
    Assignees: Trustees of Dartmouth College, Rutgers, The State University of New Jersey, The United States of America, as represented by the Secretary Department of Health and Human Services
    Inventors: Michael B. Sporn, Karen T. Liby, Gordon W. Gribble, Nanjoo Suh, Damian Medici, Pamela Gehron Robey
  • Publication number: 20140363389
    Abstract: Disclosed is a melanin production inhibitor which has an excellent inhibitory activity on the production of melanin and is highly safe. The melanin production inhibitor is represented by general formula (1) (excluding clotrimazole) and/or a pharmacologically acceptable salt thereof. In the formula, A1, A2 and A3 are independently selected from a hydrogen atom, an aryl group which may have a substituent, and an aromatic heterocyclic group which may have a substituent.
    Type: Application
    Filed: August 19, 2014
    Publication date: December 11, 2014
    Inventors: Kouji Yokoyama, Makoto Kimura, Masashi Tamai, Yuko Saitoh, Tomomi Kato, Yu Ikeda
  • Publication number: 20140343260
    Abstract: Tracers that can be used for PET or SPECT imaging of the distribution of Pgp are disclosed. The tracers are metalloprobes that can comprise a radioactive metal ion such as 67Ga or 68Ga. Methods of synthesizing the tracers, and methods of imaging heart and other tissues are also disclosed. The tracers can be used to obtain high signal-to-background ratios for imaging tissues in vivo such as heart or tumor tissue. In various embodiments, disclosed tracers can exhibit, a) enhanced first pass extraction into heart tissue compared to presently available probes, b) linearity with true blood flow, c) enhanced detection of myocardial viability compared to presently available probes, d) reduced liver retention compared to presently available probes, and e) more efficient clearance from non-cardiac and adjoining tissues compared to presently available probes.
    Type: Application
    Filed: February 10, 2012
    Publication date: November 20, 2014
    Applicant: WASHINGTON UNIVERSITY
    Inventors: Vijay Sharma, Jothilingam Sivapackiam, David Piwnica-Worms
  • Patent number: 8883800
    Abstract: The present invention relates to substituted quinazolines of formula (I): wherein X and Y are defined as in claim 1, the tautomers, stereoisomers, mixtures and salts thereof, which have valuable pharmacological properties, particularly an inhibitory effect on the activity of the enzyme dipeptidylpeptidase-IV (DPP-IV).
    Type: Grant
    Filed: July 13, 2012
    Date of Patent: November 11, 2014
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Waldemar Pfrengle, Markus Frank, Thomas Klein
  • Patent number: 8883180
    Abstract: The invention relates to active compound combinations, in particular a fungicidal and/or insecticidal composition, comprising Isotianil (3,4-dichloro-N-(2-cyanophenyl)-5-isothiazolecarboxamide) and at least one further insecticide of the anthranilamide group and optionally one further insecticide of the neonicotinoids. Moreover, the invention relates to a method for curatively or preventively controlling the phytopathogenic fungi and/or microorganisms and/or pests of plants or crops, to the use of a combination according to the invention for the treatment of seed, to a method for protecting a seed and not at least to the treated seed.
    Type: Grant
    Filed: August 29, 2013
    Date of Patent: November 11, 2014
    Assignee: Bayer Intellectual Property GmbH
    Inventors: Lutz Assmann, Ulrike Wachendorff-Neumann, Peter Dahmen, Heike Hungenberg, Wolfgang Thielert
  • Patent number: 8877793
    Abstract: The present invention is directed to the treatment of skin erythema as exhibited in rosacea and other conditions characterized by increased erythema (redness) of the skin. These conditions exhibit dilation of blood vessels due to a cutaneous vascular hyper-reactivity. In particular, the present invention is directed to a novel composition and method for the treatment of skin erythema using ?1-adrenergic receptor (?1-adrenoceptor) agonists incorporated into cosmetic, pharmacological or dermatological compositions for topical application to the skin.
    Type: Grant
    Filed: October 11, 2010
    Date of Patent: November 4, 2014
    Assignee: Allergan, Inc.
    Inventors: Stuart D. Shanler, Andrew Ondo
  • Patent number: 8864848
    Abstract: The invention relates to agents for coloring keratinic fibers, in particular human hair, including in a cosmetic carrier at least one compound of the formula (I). The structures the of the general formula (I) have a heterocycle A which bears a quaternary nitrogen atom and thus a positive charge. The invention furthermore relates to the use of these novel azo dyes in agents for coloring hair and to the dyes themselves.
    Type: Grant
    Filed: May 5, 2014
    Date of Patent: October 21, 2014
    Assignee: Henkel AG & Co. KGAA
    Inventors: Wibke Gross, Ralph Nemitz, Melanie Moch
  • Patent number: 8864849
    Abstract: The present specification provides for an agent for coloring keratinic fibers. The agent includes, a cosmetic carrier, a compound of formula (I), R1 and R2 independently of one another denote hydrogen, a C1-C6 alkyl group, a C2-C6 alkenyl group, a hydroxyl group, a halogen, a C1-C6 alkoxy group, an amino group, a nitro group, an acetyl amino group, or a sulfonamide group; or when in ortho-position to one another, form a 5- or 6-membered, saturated or unsaturated ring, which optionally include further heteroatoms.
    Type: Grant
    Filed: May 6, 2014
    Date of Patent: October 21, 2014
    Assignee: Henkel AG & Co. KGaA
    Inventors: Wibke Gross, Ralph Nemitz, Melanie Moch, Astrid Kroos, Antje Gebert
  • Patent number: 8859599
    Abstract: The present invention concerns compounds of general formula (I): Method of preparation and uses thereof.
    Type: Grant
    Filed: February 11, 2010
    Date of Patent: October 14, 2014
    Assignees: CNR—Consiglio Nazionale delle Ricerche, Istituto Scientifico Romagnolo per lo Studio e la Cura dei Tumori (I.R.S.T.) S.r.l.
    Inventors: Greta Varchi, Andrea Guerrini, Anna Tesei, Giovanni Brigliadori
  • Patent number: 8841281
    Abstract: The present invention relates to the fields of chemistry and pharmaceuticals. Embodiments of the present invention provide transition metal complexes of amino acids. Transition metal complexes of embodiments of the invention according to Categories I, II, III, and/or IV may be used as antimicrobial, anti-malarial, and anti-cancer agents, as well as catalysts in chemical reactions. Such compounds of the invention are particularly useful for combating multi-drug resistance against a broad range of microbials (such as MRSA and mycobacteria), including gram positive and gram negative bacteria, as well as can be used as anti-cancer agents against bladder cancer, breast cancer, colon cancer, rectal cancer, endometrial cancer, kidney cancer, leukemia, lung cancer, melanoma, non-Hodgkin's lymphoma, pancreatic cancer, prostate cancer, and thyroid cancer, to name a few.
    Type: Grant
    Filed: October 17, 2012
    Date of Patent: September 23, 2014
    Assignee: Virginia Tech Intellectual Properties, Inc.
    Inventor: Joseph S. Merola
  • Patent number: 8765083
    Abstract: This invention provides novel compositions comprising substituted polyamines as acid gas scrubbing solutions and methods of using the compositions in an industrial system. The invention relates to the use of such polyamine compounds in industrial processes to remove acidic contaminants from natural and industrial fluid streams, such as natural gas, combustion gas, natural gas, synthesis gas, biogas, and other industrial fluid streams. The compositions and methods of the invention are useful for removal, absorption, or sequestration of acidic contaminants and sulfide contaminants including CO2, H2S, RSH, CS2, COS, and SO.
    Type: Grant
    Filed: November 19, 2010
    Date of Patent: July 1, 2014
    Assignee: Nalco Company
    Inventors: Alan M. Blair, Keith N. Garside, William J. Andrews, Kailas B. Sawant
  • Patent number: 8697884
    Abstract: A method of manufacturing cyclic carbonate comprises a step of “preparation,” by preparing an ionic liquid polymer; and a step of “cyclization,” by feeding carbon dioxide and epoxide into a reactor containing the ionic liquid polymer to conduct a cyclization of the carbon dioxide and the epoxide in a batch or continuous reaction manner under the catalysis of the ionic liquid polymer, and finally to produce cyclic carbonate.
    Type: Grant
    Filed: April 13, 2012
    Date of Patent: April 15, 2014
    Assignee: I-Shou University
    Inventor: Shiey-Shiun Horng
  • Patent number: 8697911
    Abstract: The present invention relates to compounds of formula (I): and pharmaceutically acceptable salts thereof, wherein R1 and R2 are as defined herein. The invention also relates to pharmaceutical compositions comprising these compounds, methods of using these compounds in the treatment of various diseases and disorders, processes for preparing these compounds and intermediates useful in these processes.
    Type: Grant
    Filed: June 29, 2011
    Date of Patent: April 15, 2014
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Brian Nicholas Cook, Jennifer A. Kowalski, Xiang Li, Daniel Richard Marshall, Sabine Schlyer, Robert Sibley, Lana Louise Smith-Keenan, Fariba Soleymanzadeh, Ronald John Sorcek, Erick Richard Roush Young, Yunlong Zhang
  • 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
  • Patent number: 8685369
    Abstract: One aspect of the invention relates to complexes of a radionuclide with various heteroaryl ligands, e.g., imidazolyl and pyridyl ligands, and their use in radiopharmaceuticals for a variety of clinical diagnostic and therapeutic applications. Another aspect of the invention relates to imidazolyl and pyridyl ligands that form a portion of the aforementioned complexes. Methods for the preparation of the radionuclide complexes are also described. Another aspect of the invention relates to imidazolyl and pyridyl ligands based on derivatized lysine, alanine and bis-amino acids for conjugation to small peptides by solid phase synthetic methods. Additionally, the invention relates to methods for imaging regions of a mammal using the complexes of the invention.
    Type: Grant
    Filed: February 14, 2005
    Date of Patent: April 1, 2014
    Assignee: Molecular Insight Pharmaceuticals, Inc.
    Inventors: John Babich, Kevin Maresca, James Kronauge
  • Patent number: 8642634
    Abstract: Disclosed are compounds of Formulae 1, 1A, 1B and 1C including all geometric and stereoisomers, N-oxides, and salts thereof, wherein R1, R2, R4a1, R4a2, A, Aa, G, M, W, Z1, Z3, X, J, J1 and n are as defined in the disclosure. Also disclosed are compositions containing the compounds of Formula 1 and methods for controlling plant disease caused by a fungal pathogen comprising applying an effective amount of a compound or a composition of the invention.
    Type: Grant
    Filed: July 27, 2007
    Date of Patent: February 4, 2014
    Assignee: E I du Pont de Nemours and Company
    Inventors: Robert James Pasteris, Mary Ann Hanagan
  • Patent number: 8632914
    Abstract: The present disclosure relates to certain new and known triazolium and/or imidazolium salts and to their therapeutic use, for example in methods of treating or preventing an infection by a Plasmodium or Babesia parasite in a subject in need thereof. The triazolium and imidazolium salts are compounds of the Formula (I) or (II): wherein R1-R4, R1?-R3?, R8-R11, X, X?, X?, Y, Y? and Y? are as defined in the disclosure.
    Type: Grant
    Filed: September 4, 2009
    Date of Patent: January 21, 2014
    Assignee: University Health Network
    Inventors: Ian E. Crandall, Walter A. Szarek, Jason Z. Vlahakis
  • Patent number: 8618144
    Abstract: The present invention provides compounds of Formula (I), pharmaceutical compositions thereof, and method of using the same in the treatment or prevention of diseases mediated by the activation of ?3-adrenoceptor.
    Type: Grant
    Filed: April 28, 2010
    Date of Patent: December 31, 2013
    Assignee: Merck Sharp & Dohme Corp
    Inventors: Peter Lin, Lehua Chang, Scott D. Edmondson
  • Patent number: 8609839
    Abstract: Camphor-derived compounds are disclosed, which are represented as the following formula (I): wherein R1, R2, R3, and R4 each are defined as described in the specification. In addition, a method for manufacturing the camphor-derived compounds and application thereof are disclosed.
    Type: Grant
    Filed: January 19, 2011
    Date of Patent: December 17, 2013
    Assignee: National Tsing Hua University
    Inventors: Biing-Jiun Uang, Bo-Yao Yang
  • Patent number: 8609708
    Abstract: Disclosed are nicotine-related compounds that selectively inhibit cytochrome P-450 2A6 (CYP2A6), selectively inhibit cytochrome P-450 2A13 (CYP2A13), and/or selectively modulate a nicotinic acetylcholine receptor (nAChR). Also disclosed are pharmaceutical compositions comprising a compound of the invention, as well as methods of using the pharmaceutical compositions for treating or preventing a disease or disorder associated with nicotine-ingestion, or a disease or disorder amenable to treatment by selective modulation of nAChRs.
    Type: Grant
    Filed: August 2, 2010
    Date of Patent: December 17, 2013
    Assignee: Human BioMolecular Research Institute
    Inventor: John R. Cashman
  • Patent number: 8604071
    Abstract: The present invention relates to a method for producing 1-hydroxymethyl-1,2-diphenyloxiranes from 2,3-diphenylpropenals by means of epoxidation and reduction. The formation of objectionable by-products can be suppressed in that the reduction is started before the 2,3-5 diphenylpropenal is completely converted. The hydroxymethyl diphenyloxiranes represent valuable intermediate products for producing 1-azolylmethyl-1,2-diphenyloxiranes, wherein the latter can be easily produced from said intermediate products by introducing the azolyl group.
    Type: Grant
    Filed: February 4, 2010
    Date of Patent: December 10, 2013
    Assignee: BASF SE
    Inventors: Rainer Noack, Clemens Palm, Carsten Groening, Gunter Lipowsky
  • Patent number: 8580833
    Abstract: The present invention provides imidazole derivatives of Formula (I) and pharmaceutically acceptable salts thereof. These compounds are useful in the treatment of RAGE-mediated diseases such as Alzheimer's Disease. The present invention further relates to methods for the preparation of compounds of Formula (I) and pharmaceutically acceptable salts thereof, pharmaceutical compositions comprising such compounds, and the use the such compounds and/or pharmaceutical compositions in treating RAGE-mediated diseases.
    Type: Grant
    Filed: September 23, 2010
    Date of Patent: November 12, 2013
    Assignee: TransTech Pharma, Inc.
    Inventors: David Jones, Raju Bore Gowda, Rongyuan Xie
  • Publication number: 20130296455
    Abstract: Disclosed are a dye that is excellent in solubility and heat-resistance, and a novel compound that is suitable for the dye, and specifically provides a yellow dye having a maximum absorption wavelength in the region of 420 to 470 nm. Also disclosed are a colored (alkali-developable) photosensitive composition and an optical filter using the dye, and specifically provides a color filter that does not decrease luminance and thus is preferable for an image display device such as a liquid crystal display panel. Specifically, disclosed are a novel compound represented by the following general formula (1), a dye using the compound, and a colored (alkali-developable) photosensitive composition and a color filter. The content of the above-mentioned general formula (1) is as described in the description.
    Type: Application
    Filed: December 27, 2011
    Publication date: November 7, 2013
    Applicant: ADEKA CORPORATION
    Inventors: Yosuke Maeda, Masaaki Shimizu, Koichi Shigeno
  • Patent number: 8575359
    Abstract: The invention is in general directed to acid-sensitive linkers, and methods of use thereof, such as, for example, in drug delivery methods.
    Type: Grant
    Filed: April 4, 2007
    Date of Patent: November 5, 2013
    Assignee: The Regents of the University of California
    Inventors: Jerry Yang, Seong Deok Kong, Alice Luong, Stephen Howell
  • Patent number: 8563459
    Abstract: The invention includes a fixed-bed catalyst complex that includes (i) a metal carbene catalyst, wherein the metal is platinum, and (ii) a catalyst support that includes one or more of silica, alumina and/or glass. The invention provides a fixed-bed catalyst complex that includes a catalyst complex including a carbene chosen from those represented by at least one of Formulae (I), (II), (III), and (IV): Where the vales of X and R1 to R7 are specifically defined. The complex also includes a catalyst support that comprises silica, related reaction products, and related reaction systems.
    Type: Grant
    Filed: April 30, 2010
    Date of Patent: October 22, 2013
    Assignee: Gelest Technology, Inc.
    Inventors: Gerald L. Larson, Barry C. Arkles, Rudolph A. Cameron
  • Patent number: 8541555
    Abstract: Conjugationally extended hydrazine compositions of the formula (RR2)N(H)n(NH2)n, fluorescent hydrazone compositions of the formula (RR2)NN?C(R1R2), methods of the formation of hydrazones from the reaction of conjugationally extended hydrazines with conjugationally extended carbonyls and methods of their use in assays systems are described. Use of these conjugationally extended hydrazine and oxime compositions for direct calorimetric and fluorometric assays wherein a chromophore or the fluorophore is incorporated into the linker that is positioned between a reactive linking moiety and a biotin molecule.
    Type: Grant
    Filed: April 18, 2007
    Date of Patent: September 24, 2013
    Assignee: Solulink Biosciences, Inc.
    Inventors: David A. Schwartz, Leopoldo Mendoza
  • Patent number: 8497369
    Abstract: The present invention relates to spirocyclic heterocycles of general formula (I) the tautomers, the stereoisomers, the mixtures thereof and the salts thereof, particularly the physiologically acceptable salts thereof with inorganic or organic acids, which have valuable pharmacological properties, particularly an inhibitory effect on signal transduction mediated by tyrosine kinases, the use thereof for the treatment of diseases, particularly tumoral diseases as well as benign prostatic hyperplasia (BPH), diseases of the lungs and airways, and the preparation thereof.
    Type: Grant
    Filed: February 5, 2009
    Date of Patent: July 30, 2013
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Frank Himmelsbach, Birgit Jung, Ralf Lotz
  • Patent number: 8492553
    Abstract: The present disclosure relates to compounds, compositions and methods for the treatment of hepatitis C virus (HCV) infection. Also disclosed are pharmaceutical compositions containing such compounds and methods for using these compounds in the treatment of HCV infection.
    Type: Grant
    Filed: September 7, 2012
    Date of Patent: July 23, 2013
    Assignee: Bristol-Myers Squibb Company
    Inventors: Carol Bachand, Makonen Belema, Daniel H. Deon, Andrew C. Good, Jason Goodrich, Clint A. James, Rico Lavoie, Omar D. Lopez, Alain Martel, Nicholas A. Meanwell, Van N. Nguyen, Jeffrey Lee Romine, Edward H. Ruediger, Lawrence B. Snyder, Denis R. St. Laurent, Fukang Yang, David R. Langley, Lawrence G. Hamann
  • Patent number: 8486940
    Abstract: The invention relates to novel pyrrolidine derivatives of formula (I): wherein R1, R2 and R3 are as defined herein, as inhibitors of glutaminyl cyclase (QC, EC 2.3.2.5). QC catalyzes the intramolecular cyclization of N-terminal glutamine residues into pyroglutamic acid (5-oxo-prolyl, pGlu*) under liberation of ammonia and the intramolecular cyclization of N-terminal glutamate residues into pyroglutamic acid under liberation of water.
    Type: Grant
    Filed: September 13, 2010
    Date of Patent: July 16, 2013
    Assignee: Probiodrug AG
    Inventors: Ulrich Heiser, Daniel Ramsbeck, Robert Sommer, Antje Meyer, Torsten Hoffmann, Livia Boehme, Hans-Ulrich Demuth
  • Patent number: 8487106
    Abstract: The present invention relates to a process for preparing 2-methyl-2?-phenylpropionic acid derivatives showing antihistamine activity in more simplified way, intermediate compounds and their preparation processes used therefore. According to the present invention, pharmaceutically useful 2-methyl-2?-phenylpropionic acid derivatives can be prepared with high yield and purity on industrial scale.
    Type: Grant
    Filed: December 26, 2012
    Date of Patent: July 16, 2013
    Assignee: Yuhan Corporation
    Inventors: Chun-Ho Lee, Ja-Heouk Khoo, Kyoung-Chan Kwon, Hyun Ju
  • 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: 8445526
    Abstract: The invention provides ?-2 adrenergic receptor agonist compositions and methods for treating glaucoma and other intraocular conditions. The preferred ?-2 agonist used in the inventive compositions and methods is dexmedetomidine.
    Type: Grant
    Filed: August 14, 2012
    Date of Patent: May 21, 2013
    Assignee: Glaucoma & Nasal Therapies LLC
    Inventor: Gerald Horn
  • Patent number: 8436036
    Abstract: Compounds of the formula I: including any possible stereoisomers thereof, or a pharmaceutically acceptable salt and/or solvate thereof, as well as pharmaceutical formulations and the use of compounds of formula I as HCV inhibitors.
    Type: Grant
    Filed: April 23, 2010
    Date of Patent: May 7, 2013
    Assignee: Janssen R&D Ireland
    Inventors: Samuel Dominique Demin, David McGowan, Stefaan Julien Last, Pierre Jean-Marie Bernard Raboisson
  • Patent number: 8431607
    Abstract: The invention provides compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with the activity of Cannabinoid Receptor 1 (CB1).
    Type: Grant
    Filed: December 12, 2007
    Date of Patent: April 30, 2013
    Assignee: IRM LLC, A Delaware Limited Liability Company
    Inventors: Hong Liu, Xiaohui He, Dean Phillips, Xuefeng Zhu, Kunyong Yang, Thomas Lau, Baogen Wu, Yongping Xie, Truc Ngoc Nguyen, Xing Wang
  • Patent number: 8410141
    Abstract: The invention relates to novel arylpyrroline compounds of formula (I) which have excellent insecticidal activity and which can thus be used as an insecticide.
    Type: Grant
    Filed: May 18, 2010
    Date of Patent: April 2, 2013
    Assignee: Bayer Cropscience AG
    Inventors: Tetsuya Murata, Yasushi Yoneta, Hidetoshi Kishikawa, Jun Mihara, Daiei Yamazaki, Mamoru Hatazawa, Norio Sasaki, Kei Domon, Eiichi Shimojo, Teruyuki Ichihara, Katsuhiko Shibuya, Masashi Ataka, Ulrich Görgens
  • Patent number: 8410155
    Abstract: The present invention provides compounds of Formula (I) or (II): or a stereoisomer, tautomer, pharmaceutically acceptable salt or solvate form thereof, wherein the variables A, L1, R3, R4, R8a, R11 and M are as defined herein. The compounds of Formula (I) or (II) are selective inhibitors of serine protease enzymes of the coagulation cascade and/or contact activation system; for example thrombin, factor Xa, factor XIa, factor IXa, factor VIIa and/or plasma kallikrein. In particular, it relates to compounds that are selective factor XIa inhibitors or dual inhibitors of fXIa and plasma kallikrein. This invention also relates to pharmaceutical compositions comprising these compounds and methods of treating thromboembolic and/or inflammatory disorders using the same.
    Type: Grant
    Filed: December 13, 2007
    Date of Patent: April 2, 2013
    Assignee: Bristol-Myers Squibb Company
    Inventor: Donald J. P. Pinto
  • Patent number: 8389558
    Abstract: The present invention is directed to pharmaceutical compositions comprising bendamustine and one or more amphiphilic anionic compounds and self assembled aggregates, which aggregates exhibit enhanced stability in aqueous solutions, including plasma, are disclosed. The unexpectedly enhanced stability afforded by such aggregates permits patients to be treated with bendamustine in lower and/or with less frequent dosages or to improve its therapeutic effect while using the same as presently used treatment protocol.
    Type: Grant
    Filed: July 19, 2010
    Date of Patent: March 5, 2013
    Assignee: Supratek Pharma Inc.
    Inventors: Valery Alakhov, Grzegroz Pietrzynski, Patel Kishore, Thomasz Popek
  • Patent number: 8383663
    Abstract: The present invention is directed to pharmaceutical compositions including: (a) bendamustine, (b) a first charged cyclopolysaccharide, and (c) a stabilizing agent which is a second charged cyclopolysaccharide having a charge opposite to that of the first charged cyclopolysaccharide. The composition provides unexpectedly desirable stability in reactive environments such as plasma, coupled with unexpectedly desirable anticancer activity. The compositions are suitable for injection or infusion into patients in need for treatment with bendamustine.
    Type: Grant
    Filed: February 22, 2011
    Date of Patent: February 26, 2013
    Assignee: Supratek Pharma Inc.
    Inventors: Valery Alakhov, Grzegorz Pietrzynski, Patel Kishore, Thomasz Popek
  • Patent number: 8343913
    Abstract: A method of reducing antifungal drug resistance in which Hsp inhibitors, such as Hsp90 inhibitors, are used.
    Type: Grant
    Filed: July 5, 2005
    Date of Patent: January 1, 2013
    Assignee: Whitehead Institute for Biomedical Research
    Inventors: Leah Cowen, Susan L. Lindquist
  • Patent number: 8334316
    Abstract: The present invention provides substituted di-, tri-, tetra- and penta-sulfide compounds and compositions, and methods of using the same for the treatment and/or prevention of a cell proliferative disorder. The present invention also provides methods for preparing trisulfide compounds and compositions.
    Type: Grant
    Filed: February 9, 2009
    Date of Patent: December 18, 2012
    Assignee: ACEA Biosciences, Inc.
    Inventors: Xiao Xu, Haoyun An, Xiaobo Wang
  • Patent number: 8329718
    Abstract: The present invention provides novel ureas containing N-aryl or N-heteroaryl substituted heterocycles of Formula (I): or a stereoisomer, tautomer, pharmaceutically acceptable salt or solvate form thereof, wherein the variables A, B, D and W are as defined herein. These compounds are selective inhibitors of the human P2Y1 receptor which can be used as medicaments.
    Type: Grant
    Filed: April 16, 2010
    Date of Patent: December 11, 2012
    Assignee: Bristol-Myers Squibb Company
    Inventors: Jennifer X. Qiao, Tammy C. Wang, James C. Sutton, Timur Gungor
  • Patent number: RE44338
    Abstract: This invention relates to a method of imaging amyloid deposits and to labeled compounds, and methods of making labeled compounds useful in imaging amyloid deposits. This invention also relates to compounds, and methods of making compounds for inhibiting the aggregation of amyloid proteins to form amyloid deposits, and a method of delivering a therapeutic agent to amyloid deposits.
    Type: Grant
    Filed: July 17, 2012
    Date of Patent: July 2, 2013
    Assignee: The Trustees Of The University Of Pennsylvania
    Inventors: Hank F. Kung, Mei-Ping Kung, Zhi-Ping Zhuang, Virginia M. Y. Lee, John Q. Trojanowski, Daniel M. Skovronsky
  • Patent number: RE44354
    Abstract: This invention relates to a method of imaging amyloid deposits and to labeled compounds, and methods of making labeled compounds useful in imaging amyloid deposits. This invention also relates to compounds, and methods of making compounds for inhibiting the aggregation of amyloid proteins to form-amyloid deposits, and a method of delivering a therapeutic agent to amyloid deposits.
    Type: Grant
    Filed: July 17, 2012
    Date of Patent: July 9, 2013
    Assignee: The Trustees Of The University Of Pennsylvania
    Inventors: Hank F. Kung, Mei-Ping Kung, Zhi-Ping Zhuang, Virginia M. Y. Lee, John Q. Trojanowski, Daniel M. Skovronsky