Acyclic Nitrogen Bonded Directly To The -c(=x)- (e.g., 4,5-dihalopyrrole -2 Carboxamides, Etc.) Patents (Class 548/537)
  • Patent number: 10233150
    Abstract: The present invention relates to a composition for the modulation of the activity of non-structure proteins and a compound contained therein.
    Type: Grant
    Filed: January 30, 2017
    Date of Patent: March 19, 2019
    Assignee: Eberhard Karls Universitaet Tuebingen Medizinische Fakultaet
    Inventors: Bernhard Hirt, Claus Zeyher, Corinna Gleiser, Lothar Just
  • Patent number: 10053480
    Abstract: The anti-quorum and DNA cleaving agent is directed to a ruthenium complex formulated from dichloro-(?6-p-cymene) ruthenium(II) dimer and 2-chloroquinoxaline, the complex having the formula: The reaction cleaves the dimer, leaving a half-sandwich ruthenium complex with an ?6 coordination bond to the arene ligand and an Ru—N bond attaching the chloroquinoxaline to the ruthenium complex. The agent has an anti-quorum sensing effect on bacteria, inhibiting the formation of biofilm and inhibiting bacterial virulence. The agent also binds to DNA and may cleave the DNA, e.g., at the N7 base pair of guanine, due to a hydrolytic mechanism, suggesting potential use as an anticancer or antitumor agent.
    Type: Grant
    Filed: October 11, 2017
    Date of Patent: August 21, 2018
    Assignee: KING SAUD UNIVERSITY
    Inventors: Sartaj Tabassum, Hamad A. Al-Lohedan, Hazem Ghabour, Mohd Sajid Ali, Rais Ahmad Khan, Fohad Mabood Husain
  • Patent number: 9908850
    Abstract: Novel salt forms of [R—(R*,R*)]-2-(4-fluorophenyl)-?,?-dihydroxy-5-(1-methylethyl)-3-phenyl-4-[(phenylamino)carbonyl]-1H-pyrrole-1-heptanoic acid characterized by their X-ray powder diffraction pattern and solid-state NMR spectra are described, as well as methods for the preparation and pharmaceutical composition of the same, which are useful as agents for treating hyperlipidemia, hypercholesterolemia, osteoporosis, benign prostatic hyperplasia, and Alzheimer's Disease.
    Type: Grant
    Filed: March 24, 2017
    Date of Patent: March 6, 2018
    Assignee: Pfizer Inc.
    Inventors: Joseph Francis Krzyzaniak, Jason Albert Leonard
  • Patent number: 9790177
    Abstract: Novel forms of [R—(R*,R*)]-2-(4-fluorophenyl)-?,?-Dihydroxy-5-(1-methylethyl)-3-phenyl-4-[(phenylamino)carbonyl]-1-H-pyrrole-1-heptanoic acid hemi calcium salt designated Form XX, Form XXI, Form XXII, Form XXIII, Form XXIV, Forms XXV, Form XXVI, Form XXVII, Form XXVIII, Form XXIX, and Form XXX characterized by their X-ray powder diffraction, solid state NMR, and/or Raman spectroscopy are described, as well as methods for the preparation and pharmaceutical composition of the same, which are useful as agents for treating hyperlipidemia, hypercholesterolemia, osteoporosis, benign prostatic hyperplasia (BPH) and Alzheimer's disease.
    Type: Grant
    Filed: October 4, 2016
    Date of Patent: October 17, 2017
    Assignee: Warner-Lambert Company LLC
    Inventors: George Michael Laurence, Aeri Park, Timothy Andrew Woods
  • Patent number: 9637449
    Abstract: Novel salt forms of [R—(R*,R*)]-2-(4-fluorophenyl)-?,?-dihydroxy-5-(1-methylethyl)-3-phenyl-4-[(phenylamino)carbonyl]-1H-pyrrole-1-heptanoic acid characterized by their X-ray powder diffraction pattern and solid-state NMR spectra are described, as well as methods for the preparation and pharmaceutical composition of the same, which are useful as agents for treating hyperlipidemia, hypercholesterolemia, osteoporosis, benign prostatic hyperplasia, and Alzheimer's Disease.
    Type: Grant
    Filed: March 4, 2016
    Date of Patent: May 2, 2017
    Assignee: Pfizer Inc.
    Inventors: Joseph Francis Krzyzaniak, Jason Albert Leonard
  • Patent number: 9481647
    Abstract: Novel forms of [R—(R*,R*)]-2-(4-fluorophenyl)-?,?-dihydroxy-5-(1-methylethyl)-3-phenyl-4-[(phenylamino)carbonyl]-1H-pyrrole-1-heptanoic acid hemi calcium salt designated Form XX, Form XXI, Form XXII, Form XXIII, Form XXIV, Form XXV, Form XXVI, Form XXVII, Form XXVIII, Form XXIX, and Form XXX, characterized by their X-ray powder diffraction, solid-state NMR, and/or Raman spectroscopy are described, as well as methods for the preparation and pharmaceutical composition of the same, which are useful as agents for treating hyperlipidemia, hypercholesterolemia, osteoporosis, benign prostatic hyperplasia (BPH) and Alzheimer's disease.
    Type: Grant
    Filed: October 27, 2015
    Date of Patent: November 1, 2016
    Assignee: Warner-Lambert Company LLC
    Inventors: Joseph Francis Krzyzaniak, Kevin Quackenbush
  • Patent number: 9309195
    Abstract: Novel salt forms of [R—(R*,R*)]-2-(4-fluorophenyl)-?,?-dihydroxy-5-(1-methylethyl)-3-phenyl-4-[(phenylamino)carbonyl]-1H-pyrrole-1-heptanoic acid characterized by their X-ray powder diffraction pattern and solid-state NMR spectra are described, as well as methods for the preparation and pharmaceutical composition of the same, which are useful as agents for treating hyperlipidemia, hypercholesterolemia, osteoporosis, benign prostatic hyperplasia, and Alzheimer's Disease.
    Type: Grant
    Filed: May 19, 2015
    Date of Patent: April 12, 2016
    Assignee: Pfizer Inc.
    Inventors: Joseph Francis Krzyzaniak, Jason Albert Leonard
  • Patent number: 9199932
    Abstract: Novel forms of [R—(R*,R*)]-2-(4-fluorophenyl)-?,?-dihydroxy-5-(1-methylethyl)-3-phenyl-4-[(phenylamino)carbonyl]-1H-pyrrole-1-heptanoic acid hemi calcium salt designated Form XX, Form XXI, Form XXII, Form XXIII, Form XXIV, Form XXV, Form XXVI, Form XXVII, Form XXVIII, Form XXIX, and Form XXX, characterized by their X-ray powder diffraction, solid-state NMR, and/or Raman spectroscopy are described, as well as methods for the preparation and pharmaceutical composition of the same, which are useful as agents for treating hyperlipidemia, hypercholesterolemia, osteoporosis, benign prostatic hyperplasia (BPH) and Alzheimer's disease.
    Type: Grant
    Filed: October 22, 2014
    Date of Patent: December 1, 2015
    Assignee: Warner-Lambert Company LLC
    Inventors: Joseph Francis Krzyzaniak, Kevin Quackenbush
  • Patent number: 9085526
    Abstract: The present invention relates to a process for preparing carboxylic acid esters, comprising the reaction of at least one primary monoalcohol or of a mixture of a primary monoalcohol and at least one alcohol different therefrom in the presence of a transition metal carbene complex catalyst K which has, as central atom M, at least one transition metal atom of group 8, 9 or 10 of the Periodic Table of the Elements (IUPAC) and at least one monodentate N-heterocyclic carbene ligand, in the presence of a base, wherein the catalyst K is prepared by reacting a transition metal compound V which has at least one transition metal atom of group 8, 9 or 10 of the Periodic Table of the Elements (IUPAC), but no carbene ligand, with an imidazolium salt in the presence of the primary monoalcohol and the base, the reaction being carried out without dilution.
    Type: Grant
    Filed: July 17, 2013
    Date of Patent: July 21, 2015
    Assignee: BASF SE
    Inventors: Thomas Schaub, Stefan Rüdenauer, Daniel Schneider, Rocco Paciello
  • Patent number: 9073852
    Abstract: Novel salt forms of [R—(R*,R*)]-2-(4-fluorophenyl)-?,?-dihydroxy-5-(1-methylethyl)-3-phenyl-4-[(phenylamino)carbonyl]-1H-pyrrole-1-heptanoic acid characterized by their X-ray powder diffraction pattern and solid-state NMR spectra are described, as well as methods for the preparation and pharmaceutical composition of the same, which are useful as agents for treating hyperlipidemia, hypercholesterolemia, osteoporosis, benign prostatic hyperplasia, and Alzheimer's Disease.
    Type: Grant
    Filed: July 24, 2014
    Date of Patent: July 7, 2015
    Assignee: Pfizer Inc.
    Inventors: Joseph Francis Krzyzaniak, Jason Albert Leonard
  • Patent number: 9056831
    Abstract: A process for forming amorphous atorvastatin comprising the steps of dissolving atorvastatin in a non-hydroxylic solvent and removing the solvent by freeze-drying, as well as processes of dissolving atorvastatin in a hydroxylic solvent with a solubilizing agent or an alkalizing agent or an antioxidant and removing the solvent by freeze-drying to afford amorphous atorvastatin.
    Type: Grant
    Filed: February 8, 2014
    Date of Patent: June 16, 2015
    Assignee: Pfizer Inc.
    Inventors: Antone John deBettencourt, III, Peter Robert Rose, Evgenyi Shalaev, George Joseph Quallich, Carl Bernard Ziegler
  • Publication number: 20150148360
    Abstract: The present invention provides novel compounds of Formula (I), and pharmaceutically compositions thereof. Compounds of Formula (I) are inhibitors of histone deacetylases (HDACs) and 3-hydroxy-3-methylglutaryl coenzyme A (HMG-CoA) reductase (HMGR). Also provided are methods of using the compounds and pharmaceutical compositions for inhibiting the activity of HDACs and HMGR, treating diseases associated with HDACs or HMGR (e.g., cancer, hypercholesterolemia, an acute or chronic inflammatory disease, autoimmune disease, allergic disease, pathogen infection, neurodegenerative disease, and a disease associated with oxidative stress), or inhibiting drug resistance of cancer cells.
    Type: Application
    Filed: July 19, 2013
    Publication date: May 28, 2015
    Inventors: Jung-Hsin Lin, Jim-Min Fang, Ting-Rong Chen, Jhih-Bin Chen, Ching-Chow Chen, Tzu-Tang Wei
  • Publication number: 20150141588
    Abstract: The present invention relates to curable compositions that include a hydrazide functional material (a) represented by the following Formula (I), For Formula (I): n is 2; independently for each n, x is 0 or 1, y is 0 or 1, provided that the sum of x and y is 1; L1, independently for each n, is selected from a divalent hydrocarbyl group optionally interrupted with at least one of —O— and —S—; L2, independently for each n, is selected from a divalent hydrocarbyl group; and R1, independently for each n, is selected from hydrogen and hydrocarbyl. The curable compositions further include a reactant (b) that has at least two reactive groups that are reactive with and form covalent bonds with the hydrazide groups of the hydrazide functional material (a). The present invention also relates to curable powder coating compositions and curable adhesive compositions.
    Type: Application
    Filed: November 20, 2013
    Publication date: May 21, 2015
    Applicant: PPG Industries Ohio, Inc.
    Inventors: Hongying Zhou, Tien-Chieh Chao, Shanti Swarup, Xiangling Xu
  • Publication number: 20150105378
    Abstract: The present invention provides compounds of Formula (I) or Formula (III): as defined in the specification and compositions comprising any of such novel compounds. These compounds are endothelial lipase inhibitors which may be used as medicaments.
    Type: Application
    Filed: December 18, 2014
    Publication date: April 16, 2015
    Inventors: Lynn Abell, Leonard Adam, Cullen L. Cavallaro, Heather Finlay, Todd J. Friends, Jon J. Hangeland, Ji Jiang, R. Michael Lawrence, John Lloyd, Zulan Pi, George O. Tora, Jennifer X. Qiao, Carol Hui Hu, Tammy C. Wang
  • Publication number: 20150105392
    Abstract: In one aspect, the invention relates to compounds having the formula: wherein: Ar, Z, R3, R4 and R5 are as defined in the specification, or a pharmaceutically acceptable salt thereof. These compounds have AT1 receptor antagonist activity and neprilysin inhibition activity. In another aspect, the invention relates to pharmaceutical compositions comprising such compounds; methods of using such compounds; and process and intermediates for preparing such compounds.
    Type: Application
    Filed: December 18, 2014
    Publication date: April 16, 2015
    Applicant: THERAVANCE BIOPHARMA R&D IP, LLC
    Inventors: Paul R. Fatheree, Robert Murray McKinnell
  • Publication number: 20150099786
    Abstract: The present invention relates to novel carboxamide compounds and their use for the manufacture of a medicament. The carboxamide compounds are inhibitors of calpain (calcium dependant cysteine proteases). The invention therefore also relates to the use of these carboxamide compounds for treating a disorder associated with an elevated calpain activity. The carboxamide compounds are compounds of the general formula I in which R1, R2, R3a, R3b, R4, Q, Y, A and X have the meanings mentioned in the claims and the description, the tautomers thereof and the pharmaceutically suitable salts thereof. In particular, the compounds have the general formula Ia and Ib in which R1, r, R2b, R3a, R3b, R4, Y and X have the meanings mentioned in the claims, including the tautomers thereof and the pharmaceutically suitable salts thereof.
    Type: Application
    Filed: December 15, 2014
    Publication date: April 9, 2015
    Inventors: Helmut Mack, Andreas Kling, Katja Jantos, Achim Moeller, Wilfried Hornberger, Charles W. Hutchins
  • Publication number: 20150087600
    Abstract: Provided are methods of treating a cancer characterized by the presence of a mutant allele of IDH1/2 comprising administering to a subject in need thereof a compound described here.
    Type: Application
    Filed: January 21, 2013
    Publication date: March 26, 2015
    Applicant: AGIOS PHARMACEUTICALS, INC
    Inventors: Janeta Popovici-Muller, Francesco G. Salituro, Jeffrey O. Saunders, Zhenwei Cai, Shunqi Yan, Ding Zhou
  • Patent number: 8987322
    Abstract: The present invention relates to formulations comprising therapeutically effective amounts of at least one acid-stable, carrier-mediated transport statin, at least one poorly water-soluble, carrier-mediated transport statin, or at least one large molecular weight, carrier-mediated transport statin, such as atorvastatin and rosuvastatin, or a pharmaceutically acceptable salt thereof, and methods of their use. The present formulations and methods are designed to exhibit a controlled-release of a therapeutic amount of the statin in the small intestine, thereby limiting systemic exposure of the statin and maximizing liver-specific absorption of the drug. The formulations and methods of the present invention are particularly useful for treating and/or preventing conditions that are benefited by decreasing levels of lipids and/or cholesterol in the body.
    Type: Grant
    Filed: October 19, 2004
    Date of Patent: March 24, 2015
    Assignee: Circ Pharma Research and Development Limited
    Inventors: Jackie Butler, John Devane, Paul Stark
  • Publication number: 20150080569
    Abstract: The invention is related to anti-viral compounds, compositions containing such compounds, and therapeutic methods that include the administration of such compounds, as well as to processes and intermediates useful for preparing such compounds.
    Type: Application
    Filed: June 23, 2014
    Publication date: March 19, 2015
    Applicant: Gilead Sciences, Inc.
    Inventors: Aesop Cho, Michael O'Neil Hanrahan Clarke, Choung U. Kim, John O. Link, Hyung-Jung Pyun, Xiaoning C. Sheng, Qiaoyin Wu
  • Publication number: 20150080291
    Abstract: Disclosed are peptides having biological and therapeutic activity. Particularly disclosed are lipidated di- or tri-peptides analogs of KPV or KdPT that exhibit antimicrobial activity. In particular, the peptides of this invention provide enhanced anti-microbial activity over the base tri-peptides, lysine-proline-valine and lysine-d-proline-tyrosine. The disclosed peptides have the general formula of C12-18 lipid-KXZ-NH2i wherein K is lysine; X is proline, d-proline, histidine or arginine; Z is optional and if present Z is valine, threonine, alanine or leucine; and the terminal COOH is NH2 amidated. The C12-18 lipid is preferably the lipid moiety of lauric acid (C12), myristic acid (C14), pentadecanoic acid (C15), palmitic acid (C16), or stearic acid (C18). The invention is further related to methods of using of these peptides to treat various insults, inflammations or bacterial infections affecting the skin and other related mucosal body surfaces such as the oral cavity.
    Type: Application
    Filed: March 7, 2013
    Publication date: March 19, 2015
    Inventors: Lijuan Zhang, Robin Carmichael
  • Publication number: 20150045563
    Abstract: Novel forms of [R—(R*,R*)]-2-(4-fluorophenyl)-?,?-dihydroxy-5-(1-methylethyl)-3-phenyl-4-[(phenylamino)carbonyl]-1H-pyrrole-1-heptanoic acid hemi calcium salt designated Form XX, Form XXI, Form XXII, Form XXIII, Form XXIV, Form XXV, Form XXVI, Form XXVII, Form XXVIII, Form XXIX, and Form XXX, characterized by their X-ray powder diffraction, solid-state NMR, and/or Raman spectroscopy are described, as well as methods for the preparation and pharmaceutical composition of the same, which are useful as agents for treating hyperlipidemia, hypercholesterolemia, osteoporosis, benign prostatic hyperplasia (BPH) and Alzheimer's disease.
    Type: Application
    Filed: October 22, 2014
    Publication date: February 12, 2015
    Inventors: Joseph Francis Krzyzaniak, George Michael Laurence, Aeri Park, Kevin Quackenbush, Marie Louise Reynolds, Peter Robert Rose, Timothy Andrew Woods
  • Patent number: 8951999
    Abstract: This invention relates to compounds of formula I, their use as inhibitors of the microsomal prostaglandin E2 synthase-1 (mPGES-1), pharmaceutical compositions containing them, and their use as medicaments for the treatment and/or prevention of inflammatory diseases and associated conditions such as inflammatory/nociceptive pain. A, M, R1, R2, R7, Ra, Rb, Q3, Q4, Q6, Z2, Z4, Z5, Z6 and W have meanings given in the description.
    Type: Grant
    Filed: October 20, 2010
    Date of Patent: February 10, 2015
    Assignee: Orexo AB
    Inventors: Henning Priepke, Henri Doods, Raimund Kuelzer, Roland Pfau, Dirk Stenkamp, Robert Roenn, Benjamin Pelcman
  • Patent number: 8952140
    Abstract: A compound having a structure expressed by the following General Formula (1) or a salt thereof where “R” denotes a hydrogen atom or an alkyl group.
    Type: Grant
    Filed: February 23, 2012
    Date of Patent: February 10, 2015
    Assignee: Microbial Chemistry Research Foundation
    Inventor: Shigehiro Tohyama
  • Publication number: 20150038708
    Abstract: In one aspect, the invention relates to substituted 2-hydroxy-4-(2-(phenylsulfonamido)acetamido)benzoic acid analogs, derivatives thereof, and related compounds, which are useful as inhibitors of STAT protein activity; synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating disorders of uncontrolled cellular proliferation associated with a STAT protein activity dysfunction using the compounds and compositions. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.
    Type: Application
    Filed: August 5, 2014
    Publication date: February 5, 2015
    Inventors: James Turkson, Patrick Gunning
  • Publication number: 20150031627
    Abstract: Provided are methods of treating a cancer characterized by the presence of a mutant allele of IDH1/2 comprising administering to a subject in need thereof a compound described here.
    Type: Application
    Filed: July 25, 2014
    Publication date: January 29, 2015
    Applicant: AGIOS PHARMACEUTICALS, INC
    Inventors: Rene M. Lemieux, Janeta Popovici-Muller, Jeremy Travins, Zhenwei Cai, Dawei Cui, Ding Zhou
  • Publication number: 20150031670
    Abstract: Compounds of the formula (I), in which R1, R3, R5, R6, R7, R, X and Y have the meanings indicated in Claim 1, are inhibitors of methionine aminopeptidase and can be employed for the treatment of tumours.
    Type: Application
    Filed: March 21, 2013
    Publication date: January 29, 2015
    Applicant: MERCK PATENT GmbH
    Inventors: Timo Heinrich, Frank Zenke, Mireille Krier, Manja Friese-Hamim, Jeyaprakashnarayanan Seenisamy
  • Publication number: 20150025222
    Abstract: The invention discloses new substituted anthraquinone dyes that may be useful as cellular stains. In some aspect of the invention, the nuclear stains are useful for staining the nuclei of dead or fixed cells. Another aspect of the invention relates to substituted anthraquinone dyes comprising an enzyme substrate moiety that is transformable or cleavable by an enzyme such that the transformation or cleavage of the substrate moiety causes a detectable change in the functionality or spectral properties of the dye.
    Type: Application
    Filed: April 9, 2014
    Publication date: January 22, 2015
    Applicant: Biotium, Inc.
    Inventors: Fei MAO, Wai-Yee LEUNG, Ching-Ying CHEUNG, Lori Michelle ROBERTS
  • Publication number: 20150018331
    Abstract: Antibacterial compounds of formula (I) are provided: as well as stereoisomers, pharmaceutically acceptable salts, esters, and prodrugs thereof; pharmaceutical compositions comprising such compounds; methods of treating bacterial infections by the administration of such compounds; and processes for the preparation of such compounds.
    Type: Application
    Filed: March 24, 2014
    Publication date: January 15, 2015
    Applicant: Achaogen, Inc.
    Inventors: Heinz E. Moser, Qing Lu, Phillip A. Patten, Dan Wang, Ramesh Kasar, Stephen Kaldor, Brian D. Patterson
  • Patent number: 8933115
    Abstract: The present invention is directed to statin formulations having improved solubility and/or stability and methods for the same.
    Type: Grant
    Filed: January 22, 2013
    Date of Patent: January 13, 2015
    Assignee: Cumberland Pharmaceuticals Inc.
    Inventors: Leo Pavliv, Andrew Vila
  • Patent number: 8927533
    Abstract: The present invention relates to novel amide compounds of Formula (I), and their use as anti-tumoral and pro-apoptotic agents. The invention includes the use of such compounds in medicine, in relation to cancer disease as well as other diseases where an inhibition of HDAC is responsive, and the pharmaceutical composition containing such compounds.
    Type: Grant
    Filed: September 17, 2012
    Date of Patent: January 6, 2015
    Assignee: SIGMA-TAU Industrie Farmaceutiche Riunite S.p.A.
    Inventors: Giuseppe Giannini, Walter Cabri, Gianfranco Battistuzzi, Davide Vignola, Nicola Fanto', Claudio Pisano, Loredana Vesci
  • Publication number: 20150005283
    Abstract: The present invention provides 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: Application
    Filed: February 21, 2013
    Publication date: January 1, 2015
    Applicant: Hoffmann-La Roche Inc.
    Inventors: Adrian Wai-Hing Cheung, Ryan Craig Schoenfeld, Weiya Yun, Shu-Hai Zhao
  • Publication number: 20140371451
    Abstract: The invention discloses a method for the preparation of tert-butyl 6-chloro-3,5-dioxohexanoate from Meldrum's acid derivative and its use for the preparation of tert-butyl (4R,6S)-(6-hydroxymethyl-2,2-dimethyl-1,3-dioxan-4-yl)acetate (BHA), Rosuvastatin and Atorvastatin.
    Type: Application
    Filed: August 28, 2014
    Publication date: December 18, 2014
    Inventors: Christian Noti, Guixian Hu, Barry Jackson
  • Publication number: 20140348850
    Abstract: The present invention relates to methods of reducing blood pressure in a subject by administering a plasma kallikrein inhibitor.
    Type: Application
    Filed: August 15, 2014
    Publication date: November 27, 2014
    Inventors: Edward P. Feener, Allen Clermont
  • Publication number: 20140349987
    Abstract: The invention provides modulators for the orphan nuclear receptor ROR? and methods for treating ROR? mediated diseases by administrating these novel ROR? modulators to a human or a mammal in need thereof. Specifically, the present invention provides pyrrolo carboxamide compounds of Formula (1) and the enantiomers, diastereomers, N-oxides, tautomers, solvates and pharmaceutically acceptable salts thereof.
    Type: Application
    Filed: December 3, 2012
    Publication date: November 27, 2014
    Inventors: Christoph Steeneck, Olaf Kinzel, Christian Gege, Gerald Kleymann, Thomas Hoffmann
  • Patent number: 8895758
    Abstract: Novel forms of [R—(R*,R*)]-2-(4-fluorophenyl)-?,?-dihydroxy-5-(1-methylethyl)-3-phenyl-4-[(phenylamino)carbonyl]-1H-pyrrole-1-heptanoic acid hemi calcium salt designated Form XX, Form XXI, Form XXII, Form XXIII, Form XXIV, Form XXV, Form XXVI, Form XXVII, Form XXVIII, Form XXIX, and Form XXX, characterized by their X-ray powder diffraction, solid-state NMR, and/or Raman spectroscopy are described, as well as methods for the preparation and pharmaceutical composition of the same, which are useful as agents for treating hyperlipidemia, hypercholesterolemia, osteoporosis, benign prostatic hyperplasia (BPH) and Alzheimer's disease.
    Type: Grant
    Filed: September 9, 2013
    Date of Patent: November 25, 2014
    Assignee: Warner-Lambert Company LLC
    Inventors: Joseph Francis Krzyzaniak, Kevin Quackenbush
  • Publication number: 20140335179
    Abstract: The present invention relates to micronized crystals of atorvastatin hemi-calcium, a method for the preparation of micronized crystals of atorvastatin hemi-calcium and a pharmaceutical dosage form comprising said micronized crystals of atorvastatin hemi-calcium.
    Type: Application
    Filed: June 28, 2012
    Publication date: November 13, 2014
    Applicant: DSM SINOCHEM PHARMACEUTICALS NETHERLANDS B.V.
    Inventors: Rajnish Kumar, Neeraj Tewari
  • Publication number: 20140336395
    Abstract: Novel salt forms of [R—(R*,R*)]-2-(4-fluorophenyl)-?,?-dihydroxy-5-(1-methylethyl)-3-phenyl-4-[(phenylamino)carbonyl]-1H-pyrrole-1-heptanoic acid characterized by their X-ray powder diffraction pattern and solid-state NMR spectra are described, as well as methods for the preparation and pharmaceutical composition of the same, which are useful as agents for treating hyperlipidemia, hypercholesterolemia, osteoporosis, benign prostatic hyperplasia, and Alzheimer's Disease.
    Type: Application
    Filed: July 24, 2014
    Publication date: November 13, 2014
    Inventors: Anthony Michael Campeta, Joseph Francis Krzyzaniak, Jason Albert Leonard
  • Publication number: 20140329854
    Abstract: Provided are novel heterocyclic sirtuin binding agents, e.g., N-aryl substituted pyridine dicarboxamides, which are useful as sirtuin modulators. Also provided are methods of using the pyridine dicarboxamide compounds for treating sirtuin mediated disorders and conditions, such as diabetes, cancers, and obesity and diseases related to aging.
    Type: Application
    Filed: December 12, 2012
    Publication date: November 6, 2014
    Applicant: SMB Innovation
    Inventors: Bjarne Due Larsen, Soren Andersen, Marianne Spanget Larsen
  • Publication number: 20140309193
    Abstract: There are provided inter alia compounds of formula (I) wherein R1, R2, R3, R4a and R4b are as defined in the specification and their use in therapy, especially in the treatment of bacterial (e.g. pneumococcal) infections.
    Type: Application
    Filed: December 5, 2012
    Publication date: October 16, 2014
    Inventors: Peter William Andrew, Rana Lonnen, Mafalda Pires Damaso, Fritz-Frieder Frickel, Simon Christopher Hirst, Mark William Davies, Daniel Hamza
  • Publication number: 20140302553
    Abstract: Disclosed herein is pyrroline-carboxy-lysine (PCL), a pyrrolysine analogue, which is a natural, biosynthetically generated amino acid, and methods for biosynthetically generating PCL. Also disclosed herein are proteins, polypeptides and peptides that have PCL incorporated therein and methods for incorporating PCL into such proteins, polypeptides and peptides. Also disclosed herein is the site-specific derivatization of proteins, polypeptides and peptides having PCL or pyrrolysine incorporated therein. Also disclosed herein is the crosslinking of proteins, polypeptides and peptides having PCL or pyrrolysine incorporated therein.
    Type: Application
    Filed: May 15, 2014
    Publication date: October 9, 2014
    Applicant: IRM LLC
    Inventors: Bernhard GEIERSTANGER, Weijia OU, Susan E. CELLITTI, Tetsuo UNO, Tiffany CROSSGROVE, Hsien-Po CHIU, Jan GRUNEWALD, Xueshi HAO
  • Publication number: 20140301948
    Abstract: The compounds and the synthesis of [F-18]-labeled L-glutamic acid, [F-18]-labeled L-glutamate, their derivatives as set forth in formula (I) and their uses are described.
    Type: Application
    Filed: January 13, 2014
    Publication date: October 9, 2014
    Applicant: BAYER SCHERING PHARMA AKTIENGESELLSCHAFT
    Inventors: Ludger DINKELBORG, Matthias FRIEBE, Nikolaevna Raisa KRASIKOWA, Yuri BELOKON, Fedorovna Olga KUZNETSOVA, Keith GRAHAM, Lutz LEHMANN, Mathias BERNDT
  • Patent number: 8846411
    Abstract: Levetiracetam (LEV) derivatives, methods for synthesizing LEV derivatives, and immunodiagnostic assays for LEV. The synthesis methods described herein include chirally-selective, liquid-phase synthesis steps to produce selected LEV derivatives in high-yield. LEV derivatives can include operative groups, such as: immunogenic moieties that can be used to prepare anti-LEV antibodies; antigenic moieties that can be used in immunodiagnostic assays for LEV; or tracer moieties that can be used in immunodiagnostic assays. Additionally, the LEV derivatives can be used in immunodiagnostic assays to compete with LEV for anti-LEV antibodies.
    Type: Grant
    Filed: June 9, 2010
    Date of Patent: September 30, 2014
    Assignee: Microgenics Corporation
    Inventors: Anlong Ouyang, Aniruddha Patwardhan, Lili Arabshahi
  • Patent number: 8841332
    Abstract: The present invention relates to fungicide N-(2-phenoxyethyl)carboxamide derivatives of formula (I), their aza, thia and sila analogs, their process of preparation, their use as fungicides, particularly in the form of fungicidal compositions and methods for the control of phytopathogenic fungi of plants using these compounds or their compositions. Formula (1) wherein A, T, W, X, n and Z3 to Z7 represent various substituents.
    Type: Grant
    Filed: July 30, 2009
    Date of Patent: September 23, 2014
    Assignee: Bayer Intellectual Property GmbH
    Inventors: Samir Bennabi, Jurgen Benting, Stephane Brunet, Philippe Desbordes, Peter Dahmen, Stephanie Gary, Marie-Claire Grosjean-Cournoyer, Rachel Rama, Philippe Rinolfi, Valerie Toquin, Arnd Voerste, Ulrike Wachendorff-Neumann
  • Publication number: 20140275079
    Abstract: The present invention provides for compounds of formula (I) wherein R1, R2, R3, and R10 have any of the values defined in the specification, and pharmaceutically acceptable salts thereof, that are useful as agents in the treatment of diseases and conditions, including inflammatory diseases, cancer, and AIDS. Also provided are pharmaceutical compositions comprising one or more compounds of formula (I).
    Type: Application
    Filed: March 12, 2014
    Publication date: September 18, 2014
    Inventors: Lisa A. Hasvold, John Pratt, Keith F. McDaniel, George S. Sheppard, Dachun Liu, Steven W. Elmore, Robert D. Hubbard
  • Publication number: 20140275093
    Abstract: This invention provides compounds of formula (I): wherein ring A, X1, X2, X3, R2, R4b, R10, and G have values as described in the specification, useful as inhibitors of HDAC6. The invention also provides pharmaceutical compositions comprising the compounds of the invention, and methods of using the compositions in the treatment of proliferative, inflammatory, infectious, neurological or cardiovascular diseases or disorders.
    Type: Application
    Filed: October 16, 2013
    Publication date: September 18, 2014
    Applicant: Millennium Pharmaceuticals, Inc.
    Inventors: Christopher Blackburn, Kenneth M. Gigstad, Sean J. Harrison, He Xu
  • Publication number: 20140249200
    Abstract: In various embodiments, the present invention provides methods of treating and/or preventing cardiovascular-related disease and, in particular, a method of reducing triglycerides in a subject on atorvastatin therapy, the method comprising administering to a subject in need thereof a pharmaceutical composition comprising eicosapentaenoic acid or a derivative thereof.
    Type: Application
    Filed: February 28, 2014
    Publication date: September 4, 2014
    Applicant: AMARIN PHARMACEUTICALS IRELAND LIMITED
    Inventors: Rene Braeckman, William Stirtan, Paresh Soni
  • Patent number: 8822703
    Abstract: Novel salt forms of [R—(R*,R*)]-2-(4-fluorophenyl)-?,?-dihydroxy-5-(1-methylethyl)-3-phenyl-4-[(phenylamino)carbonyl]-1H-pyrrole-1-heptanoic acid characterized by their X-ray powder diffraction pattern and solid-state NMR spectra are described, as well as methods for the preparation and pharmaceutical composition of the same, which are useful as agents for treating hyperlipidemia, hypercholesterolemia, osteoporosis, benign prostatic hyperplasia, and Alzheimer's Disease.
    Type: Grant
    Filed: September 3, 2013
    Date of Patent: September 2, 2014
    Assignee: Pfizer Inc.
    Inventors: Joseph Francis Krzyzaniak, Jason Albert Leonard
  • Patent number: 8822527
    Abstract: Disclosed herein are substituted biaryl alkyl amide compounds, methods of synthesizing substituted biaryl alkyl amide compounds and methods of treating diseases and/or conditions with substituted biaryl alkyl amide compounds.
    Type: Grant
    Filed: October 16, 2012
    Date of Patent: September 2, 2014
    Assignee: Biotheryx, Inc.
    Inventors: Kyle W. H. Chan, Frank Mercurio, David I. Stirling
  • Publication number: 20140243373
    Abstract: There is described a group of novel cyclic amine derivative compounds having an EP4 receptor agonistic activity. Specifically, the compounds according to the invention are provided with analgesic, antinflammatory, antiglaucoma activity, and also with anti-osteoporosis and antiulcerative activity. The present invention therefore relates to novel cyclic amine derivative compounds, processes for their preparation, pharmaceutical compositions containing them and their use as medicaments, inter alia for the treatment or alleviation of Prostaglandin E mediated diseases such as pain, glaucoma, ulcerative colitis and osteoporosis.
    Type: Application
    Filed: July 4, 2011
    Publication date: August 28, 2014
    Applicant: Rottapharm S.P.A.
    Inventors: Manuela Borriello, Sabrina Pucci, Luigi Piero Stasi, Lucio Rovati
  • Publication number: 20140228321
    Abstract: The present invention provides compounds of Formula (I): (I), as defined in the specification and compositions comprising any of such novel compounds. These compounds are endothelial lipase inhibitors which may be used as medicaments.
    Type: Application
    Filed: September 24, 2012
    Publication date: August 14, 2014
    Applicant: BRISTOL-MYERS SQUIBB COMPANY
    Inventors: Jennifer X. Qiao, Heather Finlay, Ji Jiang, John Lloyd, Carol Hui Hu, Zulan Pi, George O. Tora, James Neels, Jon J. Hangeland, Todd J. Friends