Chalcogen Attached Indirectly To The Six-membered Hetero Ring By Nonionic Bonding Patents (Class 546/301)
  • Patent number: 10287419
    Abstract: A rubber composition comprising a compound having one or more groups represented by formula (X) and a rubber component is provided. wherein ring W1 represents a cyclic group having at least one selected from the group consisting of —C(?O)— and —C(?S)—; N10 represents a nitrogen atom; the at least one selected from the group consisting of —C(?O)— and —C(?S)— in the ring W1 and N10 are conjugated; and Z1 represents —O— or —S—.
    Type: Grant
    Filed: November 26, 2014
    Date of Patent: May 14, 2019
    Assignee: SUMITOMO CHEMICAL COMPANY, LIMITED
    Inventors: Kazumasa Matsuo, Orhan Ozturk, Yasuo Uekita
  • Patent number: 9944612
    Abstract: Compounds of formula (I) described herein are inhibitors of the phosphodiesterase 4 (PDE4) enzyme and are useful for the prevention and/or treatment of an allergic disease state or a disease of the respiratory tract characterized by airway obstruction.
    Type: Grant
    Filed: December 5, 2013
    Date of Patent: April 17, 2018
    Assignee: Chiesi Farmaceutici S.p.A.
    Inventors: Elisabetta Armani, Gabriele Amari, Oriana Esposito, Laura Carzaniga, Carmelida Capaldi
  • Patent number: 9265768
    Abstract: The invention relates to inhibitors of the phosphodiesterase 4 (PDE4) enzyme. More particularly, the invention relates to compounds that are derivatives of 1-phenyl-2-pyridinyl alkyl alcohols, methods of preparing such compounds, compositions containing them and therapeutic use thereof.
    Type: Grant
    Filed: January 27, 2014
    Date of Patent: February 23, 2016
    Assignee: Chiesi Farmaceutici S.p.A.
    Inventors: Elisabetta Armani, Gabriele Amari, Carmelida Capaldi, Oriana Esposito, Ilaria Peretto
  • Patent number: 9102619
    Abstract: Derivatives of 1-phenyl-2-pyridinyl alkyl alcohols are useful as inhibitors of the phosphodiesterase 4 (PDE4) enzyme.
    Type: Grant
    Filed: September 25, 2014
    Date of Patent: August 11, 2015
    Assignee: CHIESI FARMACEUTICI S.P.A.
    Inventors: Maurizio Delcanale, Elisabetta Armani, Gabriele Amari
  • Patent number: 9012471
    Abstract: The present invention provides, inter alia, dihydropyridone compounds and compositions, including analogs of a vesicular monoamine transporter type 2 (VMAT2) antagonist. The present invention also provides methods of using such compounds/analogs for modulating glucose levels, and/or preventing, treating, or ameliorating the effects of diabetes and hyper-glycemia.
    Type: Grant
    Filed: April 10, 2009
    Date of Patent: April 21, 2015
    Assignee: The Trustees of Columbia University in the City of New York
    Inventors: Paul Harris, Antonella Maffei, Yuli Xie, Donald Landry
  • Patent number: 9000177
    Abstract: Derivatives of 1-phenyl-2-pyridinyl alkyl alcohols are useful as inhibitors of the phosphodiesterase 4 (PDE4) enzyme.
    Type: Grant
    Filed: January 22, 2014
    Date of Patent: April 7, 2015
    Assignee: Chiesi Farmaceutici S.p.A.
    Inventors: Maurizio Delcanale, Elisabetta Armani, Gabriele Amari
  • Patent number: 8969332
    Abstract: The present invention discloses an aryloxy dihalopropenyl ether compound with the structure shown as general formula (I), of which the group definitions can be seen in the specification. The present invention also discloses the use of the compound with general formula (I) as an insecticide in the agricultural field and an insecticidal composition using the compound with general formula (I) as an active component.
    Type: Grant
    Filed: March 28, 2012
    Date of Patent: March 3, 2015
    Assignees: Sinochem Corporation, Shenyang Research Institute of Chemical Industry Co., Ltd.
    Inventors: Changling Liu, Jichun Yang, Xiuhui Chang, Miao Li, KeKe Li, Qiao Wu, Yuquan Song
  • Patent number: 8946434
    Abstract: The present invention is directed to novel dihydropyridin-2(1H)-one compounds useful as S-nitrosoglutathione reductase (GSNOR) inhibitors and/or Neurokinin-3 (NK3) receptor antagonists, pharmaceutical compositions comprising such compounds, and methods of making and using the same.
    Type: Grant
    Filed: July 8, 2011
    Date of Patent: February 3, 2015
    Assignee: N30 Pharmaceuticals, Inc.
    Inventors: Xicheng Sun, Jian Qiu
  • Patent number: 8940902
    Abstract: A method for treating a patient suffering from disorders and deficits of the central nervous system associated with diabetes, associated with aging and neurodegeneration, comprising attention deficit disorder in general, attention deficit hyperactivity disorder (ADHD), Alzheimer's disease (AD), mild cognitive impairment, senile dementia, AIDS dementia, neurodegeneration, depression, and schizophrenia, comprising administering to a patient in need of such treatment an effective amount of a selective inhibitor of the 11-?-hydroxysteroid dehydrogenase Type 1 enzyme activity.
    Type: Grant
    Filed: July 20, 2012
    Date of Patent: January 27, 2015
    Assignee: AbbVie Inc.
    Inventors: R. Scott Bitner, Kaitlin E. Browman, Michael E. Brune, Yixian Chen, Jurgen Dinges, Karla Drescher, Peer Jacobson, Hwan-soo Jae, Ravi Kurukulasuriya, James T. Link, David J. Madar, Jyoti R. Patel, Marina A. Pliushchev, Jeffrey J. Rohde, Lynne E. Rueter, Qi Shuai, Bryan K. Sorensen, Jiahong Wang, Karsten M. Wicke, Martin Winn, Dariusz Wodka, Vince Yeh, Hong Yong
  • Publication number: 20140371232
    Abstract: Provided are cajanine structure analogous compounds, synthesis method and pharmacological effects thereof, the compounds of the present invention having the structure as represented by general formulas I, II, III, IV and V. Also provided are pharmaceutical compositions containing the compounds as active ingredient, and uses thereof; the compounds of the present invention having the pharmacological activities such as anti-virus, anti-virus-infection, nerve protection, anti-metabolic-diseases and the like. Also provided is a chemical total synthesis preparation method of the natural products cajanine, cajanine A and cajanine C. The present invention lays a foundation for the in-depth study and development of the compounds as clinical drugs in the future.
    Type: Application
    Filed: December 18, 2012
    Publication date: December 18, 2014
    Inventors: Zhuorong Li, Xingyue Ji, Situ Xue, Guanghui Zheng, Yuhuan Li, Peizhen Tao, Jiandong Jiang
  • Publication number: 20140363388
    Abstract: The present invention is directed to inhibitors of tyrosinase, pharmaceutical compositions comprising such tyrosinase inhibitors, and methods of making and using the same. Specifically, included in the present invention are compositions of matter comprised of at least one 2,4-dihydroxybenzene analog, which inhibit the activity of tyrosinase and which inhibit the overproduction of melanin.
    Type: Application
    Filed: January 13, 2014
    Publication date: December 11, 2014
    Applicant: UNIGEN, INC.
    Inventors: Sandip K. Nandy, Jiyun Liu, Alexandre Mikhailovitch Nesterov, Carmen Hertel, Abeysinghe A. Padmapriya
  • Patent number: 8840866
    Abstract: This invention relates to a method of imaging amyloid deposits and to styrylpyridine compounds, and methods of making radiolabeled styrylpyridine 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: January 7, 2013
    Date of Patent: September 23, 2014
    Assignee: The Trustees of the University of Pennsylvania
    Inventors: Hank F. Kung, Mei-Ping Kung
  • Publication number: 20140235637
    Abstract: Disclosed are compounds and methods for treating inflammatory and fibrotic disorders, including methods of modulating a stress activated protein kinase (SAPK) system with an active compound, wherein the active compound exhibits low potency for inhibition of the p38 MAPK; and wherein the contacting is conducted at a SAPK-modulating concentration that is at a low percentage inhibitory concentration for inhibition of the p38 MAPK by the compound. Also disclosed are derivatives and analogs of pirfenidone, useful for modulating a stress activated protein kinase (SAPK) system.
    Type: Application
    Filed: April 28, 2014
    Publication date: August 21, 2014
    Applicant: InterMune, Inc.
    Inventors: Karl Kossen, Scott D. Seiwert, Vladimir Serebryany, Donald Ruhrmund, Leonid D. Beigelman, Luca Francesco Mario Raveglia, Stefania Vallese, Ivana Bianchi, Tao Hu
  • Publication number: 20140235677
    Abstract: Disclosed herein are substituted N-Aryl pyridinone fibrotic inhibitors and/or collagen infiltration modulators of Formula I, process of preparation thereof, pharmaceutical compositions thereof, and methods of use thereof.
    Type: Application
    Filed: April 30, 2014
    Publication date: August 21, 2014
    Applicant: Auspex Pharmaceuticals, Inc.
    Inventors: Thomas G. Gant, Sepehr Sarshar
  • Publication number: 20140228310
    Abstract: Disclosed are methods of modulating a stress activated protein kinase (SAPK) system with an active compound, wherein the active compound exhibits low potency for inhibition of at least one p38 MAPK; and wherein the contacting is conducted at a SAPK-modulating concentration that is at a low percentage inhibitory concentration for inhibition of the at least one p38 MAPK by the compound. Also disclosed are derivatives of pirfenidone. These derivatives can modulate a stress activated protein kinase (SAPK) system.
    Type: Application
    Filed: April 28, 2014
    Publication date: August 14, 2014
    Applicant: InterMune, Inc.
    Inventors: Lawrence M. Blatt, Scott D. Seiwert, Leonid D. Beigelman, Ramachandran Radhakrishnan, Karl Kossen, Vladimir Serebryany
  • Patent number: 8795700
    Abstract: New pesticidal compositions comprising pyriproxyfen and methyl esters of C16-C18 fatty acids and having low volatile organic compound (VOC) content are provided. Methods of use and ready-to-use products are also provided.
    Type: Grant
    Filed: April 29, 2009
    Date of Patent: August 5, 2014
    Assignee: Valent U.S.A., Corporation
    Inventors: Evelyn Jean Taylor, Humberto Benito Lopez
  • Publication number: 20140187786
    Abstract: Compounds that are 1,3,4-trisubstituted benzenes which modulate (e.g., inhibit) the activity of ?-secretase. The compounds are expected to reduce the level of A?42 in patients and be useful in the treatment of diseases (e.g., Alzheimer's disease) characterized by elevated levels of A?42 and/or the formation of A? plaques.
    Type: Application
    Filed: July 18, 2013
    Publication date: July 3, 2014
    Applicant: EnVivo Pharmaceuticals, Inc.
    Inventors: Gideon Shapiro, Richard Chesworth
  • Patent number: 8741936
    Abstract: Disclosed are methods of modulating a stress activated protein kinase (SAPK) system with an active compound, wherein the active compound exhibits low potency for inhibition of at least one p38 MAPK; and wherein the contacting is conducted at a SAPK-modulating concentration that is at a low percentage inhibitory concentration for inhibition of the at least one p38 MAPK by the compound. Also disclosed are derivatives of pirfenidone. These derivatives can modulate a stress activated protein kinase (SAPK) system.
    Type: Grant
    Filed: June 20, 2012
    Date of Patent: June 3, 2014
    Assignee: Intermune, Inc.
    Inventors: Lawrence M. Blatt, Scott D. Seiwert, Leonid Beigelman, Ramachandran Radhakrishnan, Karl Kossen, Vladimir Serebryany
  • Patent number: 8715761
    Abstract: A method of providing a range of flavors to an orally-receivable or ingestible product, the method including adding at least one compound, including salts thereof, of the formula: wherein R1 may be H, OH, O(CH2)2OH, OCH2OCH3 or R2 may be selected from a range of 5- and 6-membered heterocyclic rings, and wherein R3 may be H or OH. The compounds give rise to a wide range of flavors, and some are useful as sweetness enhancers, this allowing sweetener content to be reduced while maintaining sweetness. Also disclosed are orally-receivable or ingestible products including the compounds.
    Type: Grant
    Filed: June 7, 2010
    Date of Patent: May 6, 2014
    Assignee: Givaudan S.A.
    Inventors: Andrew Daniher, Yili Wang
  • Publication number: 20140121187
    Abstract: Disclosed are 1,3-Dioxoindene derivatives, pharmaceutically acceptable salts thereof or enantiomers, a preparation method thereof, and a pharmaceutical composition for the prevention or treatment of viral diseases, comprising the same as an active ingredient. The 1,3-Dioxoindene derivatives have excellent inhibitory activity against picornaviruses including coxsackie-, entero-, echo-, Polio-, and rhinoviruses, as well as exhibiting low cytotoxicity, so that they can be useful as an active ingredient of a pharmaceutical composition for the prevention or treatment of viral diseases including poliomyelitis, paralysis, acute hemorrhagic conjunctivitis, viral meningitis, hand-foot-and-mouth disease, vesicular disease, hepatitis A, myositis, myocarditis, pancreatitis, diabetes, epidemic myalgia, encephalitis, flu, herpangina, foot-and-mouth disease, asthma, chronic obstructive pulmonary disease, pneumonia, sinusitis or otitis media.
    Type: Application
    Filed: June 18, 2012
    Publication date: May 1, 2014
    Applicants: KATHOLIEKE UNIVERSITEIT LEUVEN K.U. LEUVEN R & D, KOREA RESEARCH INSTITUTE OF CHEMICAL TECHNOLOGY
    Inventors: Young Sik Jung, Chong Kgo Lee, Ihl Young Choi, Hae Soo Kim, Pil Ho Kim, Soo Bong Han, Johan Neyts, Hendrik Jan Thibaut
  • Publication number: 20140121246
    Abstract: GPR120 agonists are provided. These compounds are useful for the treatment of metabolic diseases, including Type II diabetes and diseases associated with poor glycemic control.
    Type: Application
    Filed: October 15, 2013
    Publication date: May 1, 2014
    Applicant: Metabolex, Inc.
    Inventors: Dong Fang Shi, Jiangao Song, Christopher J. Rabbat, Jingyuan Ma, Aaron Novack, Imad Nashashibi, Xin Chen
  • Patent number: 8680288
    Abstract: The present invention relates to Pyridin-2-yl sulfanyl acid ester compounds having antiinflammatory properties. The present invention particularly relates to novel anti-inflammatory heterocyclic acid esters of Pyridin-2-yl sulfanyl having the structure of general formula 1 which have been screened for their antiinflammatory activity with respect to inhibition of adhesion of neutrophils, isolated from human peripheral blood, onto the surface of human umbilical vein endothelial cells (HU-VEC) as a result of inhibition of the cytokine-stimulated expression of cell adhesion molecule ICAM-1. The compound RS—Z, 3-(Pyridin-2-yl sulfanyl)-propionic acid pentyl ester (structure 1a, R1=H, R2=H, R3=CH2-COOC5H11) was found to be most effective for ICAM-1 and neutrophil adhesion inhibition and was found to effectively alleviate inflammation mediated by excessive leukocyte infiltration leading to inflammatory disorders or like conditions, such as acute lung injury and acute respiratory distress syndrome in mice.
    Type: Grant
    Filed: July 20, 2011
    Date of Patent: March 25, 2014
    Assignee: Council of Scientific & Industrial Research
    Inventors: Jadab Chandra Sarma, Dilip Chandra Bora, Paruchuri Gangadhar Rao, Balaram Ghosh, Sakshi Balwani
  • Patent number: 8669209
    Abstract: Soluble granule formulations of amine salts of pyridine containing carboxylic acids with improved handling properties are provided by an improved process in which the pyridine containing carboxylic acid is partially neutralized with an amine.
    Type: Grant
    Filed: November 22, 2010
    Date of Patent: March 11, 2014
    Assignee: Dow AgroSciences, LLC.
    Inventors: Franklin N. Keeney, Neil A. Foster, Martin C. Logan, Maria G. Perry
  • Patent number: 8642629
    Abstract: The invention is concerned with the compounds of formula I: and pharmaceutically acceptable salts and esters thereof, wherein W, X, Y, and R1-R7 are defined in the detailed description and claims. In addition, the present invention relates to methods of manufacturing and using the compounds of formula I as well as pharmaceutical compositions containing such compounds. The compounds of formula I are antagonists or partial agonists at the CRTH2 receptor and may be useful in treating diseases and disorders associated with that receptor such as asthma.
    Type: Grant
    Filed: November 9, 2009
    Date of Patent: February 4, 2014
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Li Chen, Fariborz Firooznia, Paul Gillespie, Yun He, Tai-An Lin, Eric Mertz, Sung-Sau So, HongYing Yun, Zhenshan Zhang
  • Publication number: 20130327251
    Abstract: Novel tridentate-, bidentate-, and monodentate-based aromatic adsorbates including self-assembled monolayers (SAMs), especially, mixed multi-component SAMs, where the adsorbates comprise an aromatic ring including one head group or a plurality of dentate head groups and one tunable tail group or a plurality of tail groups and methods for making the same, and methods for using same, their use in the preparation of homogeneously mixed multi-component self-assembled monolayers (SAMs). The adsorbants and SAMs derived therefrom are ideally suited for biosensing, biosensing diagnostics, biological interfacial mimics, surface protections for nanoparticles, inert coatings for artificial implants, and corrosion-resistant coatings for microelectronics components.
    Type: Application
    Filed: March 7, 2013
    Publication date: December 12, 2013
    Applicant: THE UNIVERSITY OF HOUSTON SYSTEM
    Inventors: T. Randall Lee, Supachai Rittikulsittichai, Thomas Frank, Burapol Singhana
  • Publication number: 20130281387
    Abstract: Provided herein are methods for treating conditions associated with a chemosensory receptor, including diabetes, obesity, and other metabolic diseases, disorders or conditions by administering a composition comprising a chemosensory receptor ligand. Also provided herein are chemosensory receptor ligand compositions and methods for the preparation thereof for use in the methods of the present invention.
    Type: Application
    Filed: October 18, 2011
    Publication date: October 24, 2013
    Applicant: ELCELYX THERAPEUTICS, INC.
    Inventors: Alain D. Baron, Martin R. Brown, Christopher R.G. Jones, Nigel R.A. Beeley
  • Patent number: 8563583
    Abstract: MCHR1 antagonists are provided having the following Formula I: wherein all of the variables are defined herein. Such compounds are useful for the treatment of MCHR1 mediated diseases, such as obesity, diabetes, IBD, depression, and anxiety.
    Type: Grant
    Filed: March 9, 2010
    Date of Patent: October 22, 2013
    Assignee: Bristol-Myers Squibb Company
    Inventors: Saleem Ahmad, William N. Washburn, Andres S. Hernandez, Jeffrey A. Robl, Khehyong Ngu, Zhenghua Wang
  • Publication number: 20130202573
    Abstract: Described herein are compounds useful in the modulation of blood uric acid levels, formulations containing them and methods of using them. In some embodiments, the compounds described herein are used in the treatment or prevention of disorders related to aberrant levels of uric acid.
    Type: Application
    Filed: June 15, 2011
    Publication date: August 8, 2013
    Applicant: Ardea Biosciences, Inc.
    Inventors: Samedy Ouk, Esmir Gunic, Jean-Michel Vernier, Chixu Chen
  • Patent number: 8501658
    Abstract: This invention provides a convenient method for converting imines and other electrophiles into heterocyclic ring systems. The process does not require the use of metallic reagents, and is catalyzed by an organic heterocyclic carbene catalyst. Accordingly, it produces the desired compounds without the concomitant production of a large volume of metallic waste. Chiral heterocyclic carbene catalysts of the invention and methods of using these catalysts produce chiral heterocycles in high enantiomeric and diastereomeric excess.
    Type: Grant
    Filed: April 23, 2007
    Date of Patent: August 6, 2013
    Assignee: The Regents of the University of California
    Inventors: Jeffrey Bode, Ming He, Justin Struble
  • Patent number: 8461183
    Abstract: The present invention relates to novel PPAR agonist compounds as well as pharmaceutical compositions containing them. The compounds according to the invention are of quite particular therapeutic interest, notably for treating diabetes and/or dyslipidemias, as well as for preventing cardiovascular pathologies.
    Type: Grant
    Filed: May 26, 2009
    Date of Patent: June 11, 2013
    Assignee: Genfit
    Inventors: Christophe Masson, Karine Caumont-Bertrand
  • Patent number: 8455654
    Abstract: A nanoscale pigment particle composition includes an organic benzimidazolone pigment, and a sterically bulky stabilizer compound, wherein the benzimidazolone pigment associates non-covalently with the sterically bulky stabilizer compound that is a substituted pyridine derivative; and the presence of the associated stabilizer limits the extent of particle growth and aggregation, to afford nanoscale pigment particles.
    Type: Grant
    Filed: July 18, 2011
    Date of Patent: June 4, 2013
    Assignees: Xerox Corporation, National Research Council of Canada
    Inventors: Rina Carlini, Darren Andrew Makeiff
  • Patent number: 8449936
    Abstract: A method of providing a range of flavors to an orally-receivable or ingestible product, the method including adding at least one compound, including salts thereof, of the formula: wherein R1 may be H, OH, O(CH2)2OH, OCH2OCH3 or R2 may be selected from a range of 5- and 6-membered heterocyclic rings, and wherein R3 may be H or OH. The compounds give rise to a wide range of flavors, and some are useful as sweetness enhancers, this allowing sweetener content to be reduced while maintaining sweetness. Also disclosed are orally-receivable or ingestible products including the compounds.
    Type: Grant
    Filed: February 20, 2009
    Date of Patent: May 28, 2013
    Assignee: Givaudan SA
    Inventors: Andrew Daniher, Yili Wang
  • Publication number: 20130131056
    Abstract: The present invention relates to phenylethynyl compounds of formula I wherein R1, R2, X, L, R3, R4, R4?, cyc, and n are as defined in the specification and claims and to a pharmaceutically acceptable acid addition salt, to a racemic mixture, or to its corresponding enantiomer and/or optical isomer and/or stereoisomer thereof. Compounds of formula I are positive allosteric modulators (PAM) of the metabotropic glutamate receptor subtype 5 (mGluR5). They are useful for the treatment of schizophrenia or cognitive diseases.
    Type: Application
    Filed: January 15, 2013
    Publication date: May 23, 2013
    Applicant: Hoffmann-La Roche Inc.
    Inventor: Hoffmann-La Roche Inc.
  • Publication number: 20130131350
    Abstract: The present invention relates to Pyridin-2-yl sulfanyl acid ester compounds having antiinflammatory properties. The present invention particularly relates to novel anti-inflammatory heterocyclic acid esters of Pyridin-2-yl sulfanyl having the structure of general formula 1 which have been screened for their antiinflammatory activity with respect to inhibition of adhesion of neutrophils, isolated from human peripheral blood, onto the surface of human umbilical vein endothelial cells (HU-VEC) as a result of inhibition of the cytokine-stimulated expression of cell adhesion molecule ICAM-1. The compound RS—Z, 3-(Pyridin-2-yl sulfanyl)-propionic acid pentyl ester (structure 1a, R1=H, R2=H, R3=CH2-COOC5H11) was found to be most effective for ICAM-1 and neutrophil adhesion inhibition and was found to effectively alleviate inflammation mediated by excessive leukocyte infiltration leading to inflammatory disorders or like conditions, such as acute lung injury and acute respiratory distress syndrome in mice.
    Type: Application
    Filed: July 20, 2011
    Publication date: May 23, 2013
    Applicant: COUNCIL OF SCIENTIFIC & INDUSTRIAL RESEARCH
    Inventors: Jadab Chandra Sarma, Dilip Chandra Bora, Paruchuri Gangadhar Rao, Balaram Ghosh, Sakshi Balwani
  • Publication number: 20130096161
    Abstract: The present invention is directed to novel dihydropyridin-2(1H)-one compounds useful as S-nitrosoglutathione reductase (GSNOR) inhibitors and/or Neurokinin-3 (NK3) receptor antagonists, pharmaceutical compositions comprising such compounds, and methods of making and using the same.
    Type: Application
    Filed: July 8, 2011
    Publication date: April 18, 2013
    Applicant: N30 PHARMACEUTICALS, INC.
    Inventors: Xicheng Sun, Jian Qiu
  • Patent number: 8383826
    Abstract: Derivatives of 1-phenyl-2-pyridinyl alkyl alcohols are useful as inhibitors of the phosphodiesterase 4 (PDE4) enzyme.
    Type: Grant
    Filed: January 20, 2012
    Date of Patent: February 26, 2013
    Assignee: Chiesi Farmaceutici S.p.A.
    Inventors: Maurizio Delcanale, Elisabetta Armani, Gabriele Amari
  • Patent number: 8362041
    Abstract: Disclosed herein is a method for the production of disulfide compounds of the formula (I) PAC-SA—SB—R* (I) wherein PAC-SA is a residue of a pharmaceutically active drug a metabolite thereof or a pharmaceutically acceptable salt thereof that is covalently bonded via the sulfur atom, SA of a reduced sulfhydryl, sulfinyl, sulfonyl or sulfonamide group to the sulfur atom SB of an oxidized sulfhydryl group of a pharmacologically acceptable sulfhydryl compound in the absence of an acid. Preferably the pharmaceutically active drug is a proton pump inhibitor and the sulfhydryl compound is N-acetyl cysteine. The disulfide compounds according to the invention can be prepared either in vitro or in vivo and are stable in the acidic conditions of the stomach. Pharmaceutical compositions containing compounds of the formula (I) and a method for the treatment or prophylaxis of gastrointestinal disorders using compounds of the formula (I) are also described.
    Type: Grant
    Filed: November 17, 2006
    Date of Patent: January 29, 2013
    Assignee: JON Pty Limited
    Inventor: John Allen Hackett
  • Publication number: 20130023567
    Abstract: A compound for use in the treatment of proliferative disorders, such as cancer, having the following formula: wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R11, R12 and R13 are as defined in the specification.
    Type: Application
    Filed: July 25, 2012
    Publication date: January 24, 2013
    Applicant: Spear Therapeutics Limited
    Inventors: Gerard A. Potter, Philip Huxley, Kenneth J. Beresford
  • Publication number: 20120277180
    Abstract: Provided herein are methods and systems for identifying one or more cofactors such as vitamins for individuals based on the genetic makeup of the individual by detecting the presence or absence of at least one genetic variant, determining a predisposition to cofactor remediable condition, generating a personalized nutritional advice plan based on the genetic variant. Also provided herein are formulations of cofactors determined by the genetic make-up of the individual and methods of determining and producing these formulations.
    Type: Application
    Filed: September 30, 2010
    Publication date: November 1, 2012
    Applicants: VITAPATH GENETICS, INC, THE REGENTS OF THE UNIVERSITY OF CALIFORNIA
    Inventors: Nicholas Marini, Jasper Rine, Dennis Austin Gilbert, Bruce Cohen
  • Publication number: 20120277270
    Abstract: The present invention relates to methods and compositions of metadoxine and physiologically compatible active derivatives thereof, and their use for decreasing symptoms of alcohol consumption as well as in the prevention of alcohol consumption related symptoms in subjects in need thereof.
    Type: Application
    Filed: July 3, 2012
    Publication date: November 1, 2012
    Applicant: Alcobra Ltd.
    Inventors: Gur Megiddo, Dalia Megiddo, Rina Yamin, Yaron Ilan, Shimon Amselem
  • Publication number: 20120258924
    Abstract: Disclosed are methods of modulating a stress activated protein kinase (SAPK) system with an active compound, wherein the active compound exhibits low potency for inhibition of at least one p38 MAPK; and wherein the contacting is conducted at a SAPK-modulating concentration that is at a low percentage inhibitory concentration for inhibition of the at least one p38 MAPK by the compound. Also disclosed are derivatives of pirfenidone. These derivatives can modulate a stress activated protein kinase (SAPK) system.
    Type: Application
    Filed: June 20, 2012
    Publication date: October 11, 2012
    Applicant: INTERMUNE, INC.
    Inventors: Lawrence M. Blatt, Scott D. Seiwert, Leonid Beigelman, Ramachandran Radhakrishnan, Karl Kossen, Vladimir Serebryany
  • Patent number: 8273773
    Abstract: Compounds having the formula I wherein R1, R2, R3, R4a, R4b, R4c, R5, R6, R9 and n are as defined herein are Hepatitis C virus NS5b polymerase inhibitors. Also disclosed are compositions and methods for treating an HCV infection and inhibiting HCV replication.
    Type: Grant
    Filed: July 22, 2009
    Date of Patent: September 25, 2012
    Assignee: Roche Palo Alto LLC
    Inventors: Kenneth Albert Brameld, David Scott Carter, Elbert Chin, Javier de Vicente Fidalgo, Jim Li, Ryan Craig Schoenfeld, Eric Brian Sjogren, Francisco Xavier Talamas
  • Patent number: 8227490
    Abstract: Compounds of the formula (I) are disclosed and are suitable for the treatment of seborrheic dermatitis.
    Type: Grant
    Filed: July 7, 2011
    Date of Patent: July 24, 2012
    Assignee: Medicis Pharmaceutical Corporation
    Inventors: Manfred Bohn, Karl Theodor Kraemer, Astrid Markus
  • Publication number: 20120129812
    Abstract: Provided is a heterocyclic derivative showing a thyroid hormone ? receptor agonist action, which is effective for the prophylaxis or treatment of the diseases relating to the action. A compound represented by the formula [I]: wherein each symbol is as defined in the specification, a pharmacologically acceptable salt thereof, and a medicament containing the compound as an active ingredient.
    Type: Application
    Filed: April 19, 2010
    Publication date: May 24, 2012
    Applicant: MITSUBISHI TANABE PHARMA CORPORATION
    Inventors: Shinji Kawata, Koji Matsumoto, Maki Nijima, Taichi Takahashi
  • Publication number: 20120122784
    Abstract: The invention relates to novel calcium-sensing receptor (CaSR) modulating substituted cyclopentylene compounds represented in formula I and derivatives thereof, to said compounds for use as a medicament, to said compounds for use in therapy, to pharmaceutical compositions comprising said compounds, to methods of treating diseases with said compounds, and to the use of said compounds in the manufacture of medicaments.
    Type: Application
    Filed: May 26, 2010
    Publication date: May 17, 2012
    Applicant: LEO PHARMA A/S
    Inventors: Bjarne Nørremark, Lars Kristian Albert Blæhr, Anne Eeg Knapp, Kristoffer Månsson
  • Patent number: 8173820
    Abstract: Compounds of formula (I) and salts thereof are provided: wherein n is 0, 1, 2 or 3; R1 is selected from phenyl and pyridyl, each of which is optionally substituted by one or two groups independently selected from C1-4alkyl and halogen; and R2 is selected from H and CH3 when n is 1 and R2 is H when n is 2 or 3. Processes for preparation, pharmaceutical compositions, and uses thereof as a medicament, for example in the treatment of a disease or condition mediated by a reduction or imbalance in glutamate receptor function, such as schizophrenia or cognition impairment, are also disclosed.
    Type: Grant
    Filed: December 17, 2008
    Date of Patent: May 8, 2012
    Assignee: Glaxo Group Limited
    Inventors: Nicolas Bertheleme, Wai Ngor Chan, Jaqueline Sandra Scott, Simon E. Ward
  • Publication number: 20120022115
    Abstract: Provided herein are hydroxypyridone derivatives, for example, a compound of Formula I, and pharmaceutical compositions thereof. Also provided herein are methods of their use for treating, preventing, or ameliorating one or more symptoms of a proliferative disease.
    Type: Application
    Filed: October 7, 2011
    Publication date: January 26, 2012
    Applicant: BIOTHERYX INC.
    Inventors: Frank Mercurio, Kyle W.H. Chan
  • Publication number: 20120004381
    Abstract: A method of preparing polymer, the method comprising polymerising one or more ethylenically unsaturated monomers of formula (I) where U is selected from H, C1-C4 alkyl or halogen; V is halogen or of the form O-G where G is selected from —C(O)R1 and —R1, or V is of the form NGGa where G is as defined above and Ga is selected from H and R1, G and Ga form together with N a heterocyclic ring, or V is of the form CH2Gb where Gb is selected from H, R1, OH, OR1, NR12, PR12, P(O)R12, P(OR1)2, SR1, SOR1, and SO2R1; and where the or each R1 is independently selected from optionally substituted alkyl, optionally substituted alkenyl, optionally substituted alkynyl, optionally substituted aryl, optionally substituted heteroaryl, optionally substituted carbocyclyl, optionally substituted heterocyclyl, optionally substituted arylalkyl, optionally substituted heteroarylalkyl, optionally substituted alkylaryl, optionally substituted alkylheteroaryl, and an optionally substituted polymer chain, under the control of a RA
    Type: Application
    Filed: January 22, 2010
    Publication date: January 5, 2012
    Applicant: COMMONWEALTH SCIENTIFIC AND INDUSTRIAL RESEARCH ORGANISATION
    Inventors: Ezio Rizzardo, John Chiefari, Massimo Benaglia, San Thang, Graeme Moad
  • Publication number: 20120004187
    Abstract: The invention relates to spirocyclically substituted 1,3-propane dioxide derivatives, and to the physiologically compatible salts thereof. The invention relates to compounds of the formula I in which R1, R2, R3, R4, R5, R6, R7, R8, A and X are each defined as specified, and the physiologically compatible salts thereof. The compounds are suitable, for example, for treatment of diabetes.
    Type: Application
    Filed: July 5, 2011
    Publication date: January 5, 2012
    Applicant: SANOFI
    Inventors: Stefanie KEIL, Elisabeth DEFOSSA, Viktoria DIETRICH, Siegfried STENGELIN, Andreas HERLING, Guido HASCHKE, Thomas KLABUNDE
  • Patent number: RE43632
    Abstract: The invention relates to compounds of formula: wherein R1 is selected from the group consisting of fatty acid acyl groups of 12 to 30 carbon atoms and fatty alcohol groups of 12 to 30 carbon atoms, and wherein R2 is selected from the group consisting of H, fatty acid acyl of 12 to 30 carbon atoms and fatty alcohol groups of 12 to 30 carbon atoms, the same as or different from R1, and the residue of a nutrient, drug, or other bioactive compound, and to the use of these compounds to deliver drugs and other bioactive compounds.
    Type: Grant
    Filed: May 1, 1996
    Date of Patent: September 4, 2012
    Assignee: Scarista, Ltd.
    Inventors: David B. Horrobin, Sherri Clarkson, legal representative, Mehar Manku, Philip Knowles, Peter Redden, Andrea Pitt, Paul Bradley, Paul Wakefield, Austin McMordie