Having -c(=x)-, Wherein X Is Chalcogen, Bonded Directly To The Six-membered Hetero Ring Patents (Class 546/156)
  • Patent number: 10662192
    Abstract: The present invention relates to modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator, compositions thereof, and methods therewith. The present invention also relates to methods of treating ABC transporter mediated diseases using such modulators.
    Type: Grant
    Filed: June 12, 2018
    Date of Patent: May 26, 2020
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: Sara Hadida-Ruah, Anna Hazlewood, Peter Grootenhuis, Fredrick Van Goor, Ashvani Singh, Jinglan Zhou, Jason McCartney
  • Patent number: 10532984
    Abstract: A pyridonecarboxylic acid derivative or a salt thereof is represented by Formula (1), where R1 is hydrogen, a halogen atom, a lower alkyl group, or an amino group; R2 is —NH—R6, where R6 is hydrogen, a lower alkyl group, an amino lower alkyl group, or the like; —O—R7, where R7 is hydrogen, a lower alkyl group, or the like; —(CH2)m—R8, where R8 is an amino group or the like, m is 1, 2, 3 or 4; or a cyclic amino group of Formula (2), where Y represents NH or C—R9aR9b, where R9a and R9b are each independently hydrogen, a lower alkyl group, an amino group, a lower alkyl amino group, or the like; n and p are 1 or 2; R3 is hydrogen, a halogen atom, a lower alkyl group, or the like; R4 is hydrogen or a carboxyl group-protecting group; and R5 is hydrogen or a hydroxyl group-protecting group.
    Type: Grant
    Filed: June 14, 2017
    Date of Patent: January 14, 2020
    Assignee: WAKUNAGA PHARMACEUTICAL CO., LTD.
    Inventors: Tomohiko Kinoshita, Yasuhiro Kuramoto, Satoshi Inoue, Kouji Nishimura, Tatsuya Hirano, Mai Arai, Asuka Sakurai, Daichi Kazamori, Ayuka Sasaki
  • Patent number: 10517865
    Abstract: Disclosed herein are compounds of Formula I wherein R1, R2, X, and Y are defined herein. These compounds are type II topoisomerase inhibitors and can be used in methods for treating infections caused by gram-positive pathogens, gram-negative pathogens, and drug-resistant strains thereof.
    Type: Grant
    Filed: April 13, 2018
    Date of Patent: December 31, 2019
    Assignee: Emergent Product Development Gaithersburg Inc.
    Inventors: Patrick Roussel, Jutta Heim, Peter Schneider, Christian Bartels, Yaoquan Liu, Glenn Dale, Daniel Milligan
  • Patent number: 10329276
    Abstract: A crystalline form of a drug, ways to make it, compositions containing it and methods of treatment of diseases and inhibition of adverse physiological events using it are disclosed.
    Type: Grant
    Filed: December 18, 2017
    Date of Patent: June 25, 2019
    Assignee: ABBVIE INC.
    Inventors: Geoff G. Z. Zhang, Michael F. Bradley, David M. Barnes, Rodger Henry
  • Patent number: 10167278
    Abstract: The present invention relates to new cyclopropanecarboxamide modulators of cystic fibrosis transmembrane conductance regulator proteins, pharmaceutical compositions thereof, and methods of use thereof.
    Type: Grant
    Filed: December 27, 2015
    Date of Patent: January 1, 2019
    Assignee: Auspex Pharmaceuticals, Inc.
    Inventors: Chengzhi Zhang, Justin Chakma
  • Patent number: 9956213
    Abstract: The invention provides a chemical entity of Formula (I) wherein R1, R2, R3, Y, and n have any of the values described herein and compositions comprising such chemical entities; methods of making them; and their use in a wide range of methods, including metabolic and reaction kinetic studies, detection and imaging techniques, and radioactive treatments; and therapies, including inhibiting MAO, and MAO-B selectively, enhancing neuronal plasticity, treating neurological disorders, providing neuroprotection, treating a cognitive impairment associated with a CNS disorder, enhancing the efficiency of cognitive and motor training, providing neurorecovery and neurorehabilitation, enhancing the efficiency of non-human animal training protocols, and treating peripheral disorders (including obesity, diabetes, and cardiometabolic disorders) and their associated co-morbidities.
    Type: Grant
    Filed: May 23, 2017
    Date of Patent: May 1, 2018
    Assignee: Dart NeuroScience (Cayman) Ltd.
    Inventors: Jillian Basinger, Graeme Freestone, Varsha Gupta, Alan Kaplan, Chi Ching Mak, Benjamin Pratt, Vincent Santora, Dipanjan Sengupta, Lino Valdez
  • Patent number: 9949970
    Abstract: Disclosed are compounds of general formula A useful as potential anti-tubercular agents.
    Type: Grant
    Filed: March 1, 2016
    Date of Patent: April 24, 2018
    Assignee: COUNCIL OF SCIENTIFIC AND INDUSTRIAL RESEARCH
    Inventors: Ahmed Kamal, Rajesh Vcrnc Shetti, Ponnampalli Swapna, Shaik Azeeza, A. Malla Reddy, Inshad Ali Khan, Sheikh Tasduq Abdullah, Sandeep Sharma, Nitin Pal Kalia
  • Patent number: 9931334
    Abstract: The present invention relates to solid state forms of N-[2,4-bis(1,1-dimethylethyl)-5-hydroxyphenyl]-1,4-dihydro-4-oxoquinoline-3-carboxamide (Compound 1), pharmaceutical compositions thereof and methods therewith.
    Type: Grant
    Filed: May 2, 2017
    Date of Patent: April 3, 2018
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: Patricia Hurter, William Rowe, Christopher R. Young, Adriana Costache, Patrick R. Connelly, Mariusz Krawiec, Yuchuan Gong, Yushi Feng, Martin Trudeau
  • Patent number: 9873681
    Abstract: A crystalline form of a drug, ways to make it, compositions containing it and methods of treatment of diseases and inhibition of adverse physiological events using it are disclosed.
    Type: Grant
    Filed: November 23, 2016
    Date of Patent: January 23, 2018
    Assignee: ABBVIE INC.
    Inventors: Geoff G. Z. Zhang, Michael F. Bradley, David M. Barnes, Rodger Henry
  • Patent number: 9809551
    Abstract: Provided herein is a polymorphic form of Ivacaftor, namely APO-I, as well as processes for the preparation and pharmaceutical compositions of the same. Also, provided is a new solvate of Ivacaftor, processes for its preparation and use in the preparation of pure Ivacaftor.
    Type: Grant
    Filed: November 13, 2014
    Date of Patent: November 7, 2017
    Assignee: Apotex Inc.
    Inventors: Padiyath Mohammed Akbarali, Kintali Venkata Ramana, Heggadde Nanjunda Bhatta Shreenivasa Murthy, Sankaran Suresh Kumar, Ekkaluru Vijaya Bhaskar, Nechipadappu Sunil Kumar, Karad Manjunath
  • Patent number: 9776969
    Abstract: Disclosed are processes for preparing [(3-hydroxypyridine-2-carbonyl)amino]-alkanoic acids, derivatives, inter alia, 5-aryl substituted and 5-heteroaryl substituted [(3-hydroxypyridine-2-carbonyl]amino}acetic acids. Further disclosed are methods for making prodrugs of [(3-hydroxypyridine-2-carbonyl)-amino]acetic acids, for example, {[(3-hydroxypyridine-2-carbonyl]amino}acetic acid esters and {[3-hydroxypyridine-2-carbonyl]amino}acetic acid amides. The disclosed compounds are useful as prolyl hydroxylase inhibittors or for treating conditions wherein prolyl hydroxylase inhibition is desired.
    Type: Grant
    Filed: August 24, 2015
    Date of Patent: October 3, 2017
    Assignee: Akebia Therapeutics, Inc.
    Inventors: Christopher M. Lanthier, Boris Gorin, Jan Oudenes, Craig Edward Dixon, Alan Quigbo Lu, James Densmore Copp, John Michael Janusz
  • Patent number: 9676722
    Abstract: The present invention relates to an improved process for the preparation of Ivacaftor intermediates. The present invention is also provides industrial applicable, commercially and eco-friendly viable process for the preparation of Ivacaftor.
    Type: Grant
    Filed: August 24, 2016
    Date of Patent: June 13, 2017
    Assignee: Optimus Drugs Private Limited
    Inventors: Srinivas Reddy Desi Reddy, Dnyandev Ragho Rane, Venkata Srinivasa Rao Velivela
  • Patent number: 9670163
    Abstract: The present invention relates to solid state forms of N-[2,4-bis(1,1-dimethylethyl)-5-hydroxyphenyl]-1,4-dihydro-4-oxoquinoline-3-carboxamide (Compound 1), pharmaceutical compositions thereof and methods therewith.
    Type: Grant
    Filed: September 14, 2015
    Date of Patent: June 6, 2017
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: Patricia Hurter, William Rowe, Christopher R. Young, Adriana Costache, Patrick R. Connelly, Mariusz Krawiec, Yuchuan Gong, Yushi Feng, Martin Trudeau
  • Patent number: 9539250
    Abstract: A crystalline form of a drug, ways to make it, compositions containing it and methods of treatment of diseases and inhibition of adverse physiological events using it are disclosed.
    Type: Grant
    Filed: February 3, 2015
    Date of Patent: January 10, 2017
    Assignee: ABBVIE INC.
    Inventors: Geoff G. Z. Zhang, Michael F. Bradley, David M. Barnes, Rodger Henry
  • Patent number: 9422432
    Abstract: The present document describes a composition which comprises about 25% to about 40% (v/v) plasticizers such as 2-ethylhexyl benzoate and butyl benzyl phthalate, about 0.5% to about 2% (v/v) of monoethanolamine as degasser, about 5% to about 20% (w/w) of pH adjusting agents such as calcium carbonate and ammonium carbonate, and from about 30% to about 45% (v/v) of a phenol formaldehyde resin based adhesive comprising an epoxy consisting of epichlorohydrin. The document also describes processes of making the composition as well as methods of using the composition for the pretreatment of surfaces, for example wood surface, metal rock or plastic surfaces prior to further treatment.
    Type: Grant
    Filed: November 26, 2013
    Date of Patent: August 23, 2016
    Assignee: BRYSON PATENTS INC.
    Inventor: Bryan Christopher Farnum
  • Patent number: 9371287
    Abstract: The invention provides a process for the preparation of a compound of Formula 1, comprising coupling a carboxylic acid of Formula 2 with an aniline of Formula 3 in the presence of a coupling agent.
    Type: Grant
    Filed: May 23, 2014
    Date of Patent: June 21, 2016
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: John DeMattei, Adam R. Looker, Bobbianna Neubert-Langille, Martin Trudeau, Stefanie Roeper, Michael P. Ryan, Dahrika Milfred Yap Guerette, Brian R. Krueger, Peter D. J. Grootenhuis, Fredrick F. Van Goor, Martyn C. Botfield, Gregor Zlokarnik
  • Patent number: 9273039
    Abstract: The present disclosure provides compounds of general formula A: useful as potential anti-tubercular agents.
    Type: Grant
    Filed: September 14, 2011
    Date of Patent: March 1, 2016
    Assignee: Council of Scientific and Industrial Research
    Inventors: Ahmed Kamal, Rajesh Vcrnc Shetti, Ponnampalli Swapna, Shaik Azeeza, A Malla Reddy, Inshad Ali Khan, Sheikh Tasduq Abdullah, Sandeep Sharma, Nitin Pal Kalia
  • Patent number: 9233927
    Abstract: The subject invention provides a mixture of crystalline laquinimod sodium particles, wherein (i) 90% or more of the total amount by volume of the laquinimod sodium particles have a size of 40 microns or less or (ii) 50% or more of the total amount by volume of the laquinimod sodium particles have a size of 15 microns or less, and wherein: a) the mixture has a bulk density of 0.2 g/mL to 0.4 g/mL; b) the mixture has a tapped density of 0.40 g/mL to 0.7 g/mL; c) an amount of heavy metal in the mixture is no more than 0.002% of heavy metal relative to the amount by weight of laquinimod sodium; d) an amount of 5-chloro-4-hydroxy-1-methyl-2-oxo-1,2-dihydroquinoline (MCQ) in the mixture is no more than 0.15% relative to the amount of laquinimod sodium as measured by HPLC; e) an amount of 5-chloro-4-hydroxy-1-methyl-2-oxo-1,2-dihydroqunoline-3-carboxylic acid (MCQCA) in the mixture is no more than 0.
    Type: Grant
    Filed: March 14, 2014
    Date of Patent: January 12, 2016
    Assignee: TEVA PHARMACEUTICAL INDUSTRIES, LTD.
    Inventors: Anton Frenkel, Avital Laxer
  • Patent number: 9181192
    Abstract: This invention relates to compounds of Formula I: and pharmaceutically acceptable salts thereof. This invention also provides compositions comprising a compound of this invention and the use of such compositions in methods of treating diseases and conditions that are beneficially treated by administering a CFTR potentiator.
    Type: Grant
    Filed: September 19, 2014
    Date of Patent: November 10, 2015
    Assignee: Concert Pharmaceuticals, Inc.
    Inventor: Adam J. Morgan
  • Publication number: 20150148344
    Abstract: This application relates to chemical compounds which may act as inhibitors of, or which may otherwise modulate the activity of, a bromodomain-containing protein, including bromodomain-containing protein 4 (BRD4), and to compositions and formulations containing such compounds, and methods of using and making such compounds. Compounds include compounds of Formula I wherein R1, R2, R3, R4, R7, W, X, and Z are as described herein.
    Type: Application
    Filed: November 21, 2014
    Publication date: May 28, 2015
    Inventors: Kerim Babaoglu, Britton K. Corkey, Robert H. Jiang, David Sperandio, Hai Yang
  • Publication number: 20150126487
    Abstract: The present invention provides a compound having a cholinergic muscarinic M1 receptor positive allosteric modulator activity, and useful as a prophylactic or therapeutic drug for Alzheimer's disease, schizophrenia, pain, a sleep disorder and the like. The present invention relates to a compound represented by the formula (I): wherein R1 is an optionally substituted amino group or an optionally substituted cyclic amino group, R2 and R3 are each independently a hydrogen atom or a substituent, X is —CH? or —N?, and ring A is an optionally substituted 5- to 10-membered ring, or a salt thereof.
    Type: Application
    Filed: February 28, 2013
    Publication date: May 7, 2015
    Inventors: Hiroki Sakamoto, Takahiro Sugimoto
  • Publication number: 20150111886
    Abstract: The invention relates to a compound of formula (I) wherein A1, R1 and R2 are defined as in the description and in the claims. The compound of formula (I) can be used as a medicament.
    Type: Application
    Filed: December 22, 2014
    Publication date: April 23, 2015
    Applicant: Hoffmann-La Roche Inc.
    Inventors: Atsushi Kimbara, Uwe Grether, Matthias Nettekoven, Bernd Puellmann, Mark Rogers-Evans, Tanja Schulz-Gasch
  • Publication number: 20150099780
    Abstract: This invention relates to compounds of Formula I: and pharmaceutically acceptable salts thereof. This invention also provides compositions comprising a compound of this invention and the use of such compositions in methods of treating diseases and conditions that are beneficially treated by administering a CFTR potentiator.
    Type: Application
    Filed: September 19, 2014
    Publication date: April 9, 2015
    Inventor: Adam J. Morgan
  • Patent number: 8993767
    Abstract: The present invention relates to multiphoton activable organic compounds responding to the following formula (I). The present invention also relates to a method of synthesizing the compounds of the invention, to an aqueous solution comprising at least one compound of the invention, and to their specific uses. The present invention also concerns a method of liberating organic ligands, said method involving the step of irradiating a compound according to the invention.
    Type: Grant
    Filed: January 12, 2011
    Date of Patent: March 31, 2015
    Assignee: Centre National de la Recherche Scientifique
    Inventors: Peter Dalko, Morgane Petit, David Ogden, Francine Acher
  • Publication number: 20150087886
    Abstract: This invention relates to novel cancer treatment compositions and associated therapeutic methods. More particularly, this invention relates in part to small chemical bifunctional inhibitors of DNA replication and repair proteins Metnase and/or Intnase (also termed Gypsy Integrase, Gypsy Integrease-1, Gypsy Retransposon Integrase 1, or GIN-1) that simultaneously damage DNA, and to a therapeutic method that utilizes the inhibitors to increase the effectiveness of cancer treatment protocols, including radiation therapy. In preferred embodiments, compounds, compositions and methods of treatment of the invention are used to treat a patient suffering from leukemia (e.g. acute myeloid leukemia (AML) and related cancers.
    Type: Application
    Filed: October 9, 2014
    Publication date: March 26, 2015
    Inventors: Robert Hromas, Andrei Leitao, Tudor I. Oprea, Larry A. Sklar, Elizabeth A. Williamson, Justin Wray, Wei Wang
  • Publication number: 20150080377
    Abstract: The present invention relates to deuterium-enriched pyridinonecarboxamides and their derivatives of the formula 1, and pharmaceutically acceptable salts thereof, are partial or full agonists of serotonin (5-Hydroxytryptamine or 5-HT) receptor subtype 4 (5-HT4), and are useful compounds for the prevention and treatment of Alzheimer's disease, cognitive and memory dysfunction, mild cognition impairment, memory decline, cognitive impairment associated with schizophrenia, cognitive impairment associated with age-related dementia or Alzheimer's disease, cognitive impairment associated with post-coronary bypass surgery, attention deficit hyperactivity disorder, Obsessive compulsive disorder, depression, speech improvement in autistic children, sleep apnea in Alzheimer's patients, Age-related macular degeneration (AMD), irritable bowel syndrome, gastroesophageal reflux disease, Crohn's disease, emesis, nausea, vomiting, prokinesia, non-ulcer dyspepcia, anxiety, depression, pain, migraine, urinary incontinence, a
    Type: Application
    Filed: August 31, 2013
    Publication date: March 19, 2015
    Inventor: Daljit Singh Dhanoa
  • Patent number: 8981103
    Abstract: Provision of a stabilized crystal of 6-(3-chloro-2-fluorobenzyl)-1-[(S)-1-hydroxymethyl-2-methylpropyl]-7-methoxy-4-oxo-1,4-dihydroquinoline-3-carboxylic acid (compound A). A crystal of compound A, which shows a particular X-ray powder diffraction pattern of a characteristic diffraction peaks at diffraction angles 2?(°) as measured by X-ray powder diffractometry.
    Type: Grant
    Filed: August 10, 2009
    Date of Patent: March 17, 2015
    Assignee: Japan Tobacco Inc.
    Inventors: Koji Ando, Koji Matsuda, Shuji Miyake, Hideto Uehara
  • Publication number: 20150073015
    Abstract: The invention provides a process for the preparation of a compound of Formula 1, comprising coupling a carboxylic acid of Formula 2 with an aniline of Formula 3 in the presence of a coupling agent.
    Type: Application
    Filed: May 23, 2014
    Publication date: March 12, 2015
    Inventors: John DeMattei, Adam R. Looker, Bobbianna Neubert-Langille, Martin Trudeau, Stefanie Roeper, Michael P. Ryan, Dahrika Milfred Yap Guerette, Brian R. Krueger, Peter D.J. Grootenhuis, Fredrick F. Van Goor, Martyn C. Botfield, Gregor Zlokarnik
  • Publication number: 20150065487
    Abstract: The present invention relates to modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator, compositions thereof, and methods therewith. The present invention also relates to methods of treating ABC transporter mediated diseases using such modulators.
    Type: Application
    Filed: November 11, 2014
    Publication date: March 5, 2015
    Inventors: Sara Hadida-Ruah, Anna Hazlewood, Peter Grootenhuis, Fred Van Goor, Ashvani Singh, Jinglan Zhou, Jason McCartney
  • Patent number: 8969569
    Abstract: A crystalline form of a drug, ways to make it, compositions containing it and methods of treatment of diseases and inhibition of adverse physiological events using it are disclosed.
    Type: Grant
    Filed: February 7, 2014
    Date of Patent: March 3, 2015
    Assignee: AbbVie Inc.
    Inventors: Geoff G. Z. Zhang, Michael F. Bradley, David M. Barnes, Rodger Henry
  • Patent number: 8946430
    Abstract: The present invention provides compounds of Formula (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: Grant
    Filed: September 24, 2012
    Date of Patent: February 3, 2015
    Assignee: Bristol-Myers Squibb Company
    Inventors: Jennifer X. Qiao, Carol Hui Hu, Tammy C. Wang
  • Publication number: 20150031722
    Abstract: The present invention relates to modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator, compositions thereof, and methods therewith. The present invention also relates to methods of treating ABC transporter mediated diseases using such modulators.
    Type: Application
    Filed: October 6, 2014
    Publication date: January 29, 2015
    Inventors: Sara Hadida-Ruah, Anna Hazlewood, Peter Grootenhuis, Fredrick Van Goor, Ashvani Singh, Jinglan Zhou, Jason McCartney
  • Patent number: 8927723
    Abstract: A process for making 1-(6-amino-3,5-difluoropyridin-2-yl)-8-chloro-6-fluoro-7-(3-hydroxyazetidin-1-yl)-4-oxo-1,4-dihydro-3-quinolinecarboxylic acid, and therapeutically acceptable salts thereof, and intermediates used in the process are disclosed.
    Type: Grant
    Filed: February 10, 2014
    Date of Patent: January 6, 2015
    Assignee: AbbVie, Inc.
    Inventors: Anthony Haight, David M. Barnes, Geoff G. Z. Zhang
  • Publication number: 20150005287
    Abstract: The present invention provides a compound represented by the formula (I) wherein X is a hydrogen atom or a fluorine atom; R is a hydrogen atom or alkyl; R1 is (1) cyclopropyl optionally substituted by to 3 halogen atoms or (2) phenyl optionally substituted by 1 to 3 halogen atoms; R2 is alkyl, alkoxy, haloalkoxy, a halogen atom, cyano, etc.; and R3 is 7-oxo-7,8-dihydro-1,8-naphthyridinyl, 3-pyridyl, etc., or a salt thereof. The compound of the present invention has excellent antimicrobial activity against Clostridium difficile and is useful for the prevention or treatment of intestinal infection such as Clostridium difficile-associated diarrhea.
    Type: Application
    Filed: February 28, 2014
    Publication date: January 1, 2015
    Inventors: Mamuti ABUDUSAIMI, Fangguo YE, Jiangqin SUN, Hisashi MIYAMOTO, Jay-Fei CHENG, Daisuke OKA
  • Publication number: 20140357650
    Abstract: The present invention relates to novel inhibitors having high selectivity and specificity for FAP (fibroblast activation protein). Said inhibitors are useful as a human and/or veterinary medicine, in particular for the treatment and/or prevention of FAP-related disorders such as but not limited to proliferative disorders.
    Type: Application
    Filed: January 17, 2013
    Publication date: December 4, 2014
    Applicant: Fox Chase Cancer Center
    Inventors: Koen Jansen, Ingrid De Meester, Leen Heirbaut, Jonathan D. Cheng, Jurgen Joossens, Koen Augustyns, Pieter Van Der Veken
  • Patent number: 8884018
    Abstract: The present invention relates to processes for preparing solid state forms of N-(4-(7-azabicyclo[2.2.1]heptan-7-yl)-2-(trifluoromethyl)phenyl)-4-oxo-5-(trifluoromethyl)-1,4-dihydroquinoline-3-carboxamide, including Compound 1 Form A, Compound 1 Form A-HCl, Compound 1 Form B, and Compound 1 Form B-HCl, any combination of these forms, pharmaceutical compositions thereof, and methods of treatment therewith.
    Type: Grant
    Filed: March 7, 2014
    Date of Patent: November 11, 2014
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: Narendra Bhalchandra Ambhaikar, Robert Hughes, Dennis James Hurley, Elaine Chungmin Lee, Benjamin Littler, Mehdi Numa, Stefanie Roeper, Urvi Sheth
  • Publication number: 20140329855
    Abstract: The present invention relates to solid state forms of N-[2,4-bis(1,1-dimethylethyl)-5-hydroxyphenyl]-1,4-dihydro-4-oxoquinoline-3-carboxamide (Compound 1), pharmaceutical compositions thereof and methods therewith.
    Type: Application
    Filed: July 18, 2014
    Publication date: November 6, 2014
    Inventors: Sneha G. Arekar, Steven C. Johnston, Mariusz Krawiec, Ales Medek, Praveen Mudunuri, Mark Jeffrey Sullivan
  • Patent number: 8877752
    Abstract: Provided are 4(1H)-quinolone derivatives effective in inhibiting or eliminating the viability of at least one of the stages in the life-cycle of the malarial parasite, and to show a reduced propensity to induce resistance to the compound by the target parasite. In particular, the compounds can be derivatives of phenoxyethoxy-quinolones, and including, but not only, 7-(2-phenoxyethoxy)quinolin derivatives. These compounds may be administered by themselves, with at least one other derivative compound, or with other antimalarial compounds, to an animal or human subject. The therapeutic compositions can be and formulated to reduce the extent of a Plasmodium infection in the recipient subject, or to reduce the likelihood of the onset or establishment of a Plasmodium infection if administered prior to the parasite contacting the subject. The therapeutic compositions can be formulated to provide an effective single dose amount of an antimalarial compound or multiple doses for administering over a period of time.
    Type: Grant
    Filed: October 26, 2012
    Date of Patent: November 4, 2014
    Assignee: University of South Florida
    Inventors: Roman Manetsch, Richard Matthew Cross, Niranjan Kumar Namelikonda, Dennis Edward Kyle, Tina Susanna Mutka, Alexis Nichole LaCrue, Jordany Richarlson Maignan, Fabian Ernesto Saenz
  • Patent number: 8877931
    Abstract: The invention provides synthetic processes and synthetic intermediates that can be used to prepare 4-oxoquinolone compounds having useful integrase inhibiting properties.
    Type: Grant
    Filed: August 1, 2013
    Date of Patent: November 4, 2014
    Assignee: Gilead Sciences, Inc.
    Inventors: Dominika Pcion, Carrie Tomasi, Mark Charles Whitcomb, Eric D. Dowdy, Wenyi Fu, Patricia MacLeod
  • Patent number: 8865902
    Abstract: This invention relates to compounds of Formula I: and pharmaceutically acceptable salts thereof. This invention also provides compositions comprising a compound of this invention and the use of such compositions in methods of treating diseases and conditions that are beneficially treated by administering a CFTR potentiator.
    Type: Grant
    Filed: November 18, 2013
    Date of Patent: October 21, 2014
    Assignee: Concert Pharmaceuticals, Inc.
    Inventor: Adam J. Morgan
  • Publication number: 20140303204
    Abstract: The present invention relates to modulators of cystic fibrosis transmembrane conductance regulator (“CFTR”), compositions thereof, and methods therewith. The present invention also relates to methods of treating diseases using modulators of CFTR.
    Type: Application
    Filed: June 6, 2014
    Publication date: October 9, 2014
    Applicant: Vertex Pharmaceuticals Incorporated
    Inventors: Hayley Binch, Lev T.D. Fanning, Dennis Hurley, Urvi Sheth, Alina Silina, Xiaoqing Yang, Martyn Botfield, Peter D.J. Grootenhuis, Fredrick Van Goor, Mehdi Michel Djamel Numa
  • Publication number: 20140303150
    Abstract: The invention relates to compounds of general formula I wherein R is heteroaryl optionally substituted by R7; or R is heterocycloalkyl or heterocycloalkenyl, optionally substituted by R8; or R is X wherein X is —NR11R12; and pharmaceutically acceptable salts, hydrates, or solvates thereof, for use—alone or in combination with one or more other pharmaceutically active compounds—in therapy, for preventing, treating or ameliorating diseases or conditions responsive to stimulation of neutrophil oxidative burst, responsive to stimulation of keratinocyte IL-8 release or responsive to induction of necrosis.
    Type: Application
    Filed: December 22, 2011
    Publication date: October 9, 2014
    Applicant: LEO Laboratories Limited
    Inventors: Gunnar Grue-Sørensen, Xifu Liang, Thomas Högberg, Kristoffer Månsson, Per Vedsø, Thomas Vifian
  • Publication number: 20140303205
    Abstract: This invention relates to a compound of Formula I: or a pharmaceutically acceptable salt thereof, wherein R is COOH or CH2OH.
    Type: Application
    Filed: June 20, 2014
    Publication date: October 9, 2014
    Inventors: Xiaoqing Yang, Sara Sabina Hadida Ruah, Peter Diederik Jan Grootenhuis, Fredrick F. Van Goor, Martyn Curtis Botfield, Gregor Zlokarnik
  • Publication number: 20140288310
    Abstract: Disclosed is a technique for improving the water solubility and storage stability of 7-{(3S,4S)-3-[(cyclopropylamino)methyl]-4-fluoropyrrolidine-1-y1}-6-fluoro-1-(2-fluoroethyl)-8-methoxy-4-oxo-1,4-dihydroquinoline-3-carboxylic acid (compound (1)) that is safe and not only has a strong antibacterial action but also is effective for resistant bacteria for which conventional antibacterial agent are less effective. Crystals of the hydrochloride salt of the compound (1), crystals of the hydrochloride salt hydrate of the compound (1), and crystals of the methanesulfonate salt of the compound (1) are provided. In these crystals, decomposition due to influences of light is suppressed as compared to that in crystals of the compound (1) in free, and their storage stability is high. These crystals have higher solubility in water than the crystals of the compound (1) in free.
    Type: Application
    Filed: November 9, 2012
    Publication date: September 25, 2014
    Applicant: KYORIN PHARMACEUTICAL CO., LTD
    Inventors: Ichiro Araya, Akinori Goto, Wataru Minagawa, Keiko Funada, Muneki Nagao
  • Patent number: 8841321
    Abstract: Use of a compound for the manufacture of a medicament for the treatment of a bacterial infection provided that the bacterial infection is other than a Mycobacterial infection, said compound being a compound of formula (Ia) or (Ib) a pharmaceutically acceptable acid or base addition salt thereof, a stereochemically isomeric form thereof, a tautomeric form thereof or a N-oxide form thereof, wherein R1 is hydrogen, halo, haloalkyl, cyano, hydroxy, Ar, Het, alkyl, alkyloxy, alkylthio, alkyloxyalkyl, alkylthioalkyl, Ar-alkyl or di(Ar)alkyl; p is 1, 2, 3 or 4; R2 is hydrogen, hydroxy, mercapto, alkyloxy, alkyloxyalkyloxy, alkylthio, mono or di(alkyl)amino or a radical of formula; R3 is alkyl, Ar, Ar-alkyl, Het or Het-alkyl; q is 1, 2 or 3; R4 and R5 are hydrogen, alkyl or benzyl; or R4 and R5 together and including the N to which they are attached may form a ring; R6 is hydrogen, halo, haloalkyl, hydroxy, Ar, alkyl, alkyloxy, alkylthio, alkyloxyalkyl, alkythioalkyl, Ar-alkyl or di(Ar)alkyl; or two vicinal R6 radica
    Type: Grant
    Filed: June 26, 2006
    Date of Patent: September 23, 2014
    Assignee: Janssen Pharmaceutica NV
    Inventors: Koenraad Jozef Lodewijk Marcel Andries, Anil Koul, Jérôme Emile Georges Guillemont, David Francis Alain Lançois, Magali Madeleine Simone Motte, Ismet Dorange, Leo Jacobus Jozef Backx, Lieven Meerpoel
  • Patent number: 8835639
    Abstract: The invention provides a process for the preparation of a compound of Formula 1, comprising coupling a carboxylic acid of Formula 2 with an aniline of Formula 3 in the presence of a coupling agent.
    Type: Grant
    Filed: November 6, 2012
    Date of Patent: September 16, 2014
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: John DeMattei, Adam R. Looker, Bobbianna J. Neubert-Langille, Martin Trudeau, Stefanie Roeper, Michael P. Ryan, Dahrika Milfred Yap Guerette, Brian R. Krueger, Peter Diederik Jan Grootenhuis, Fredrick F. Van Goor, Martyn Curtis Botfield, Gregor Zlokarnik
  • Publication number: 20140256770
    Abstract: The invention provides a process for the preparation of a compound of Formula 1, comprising coupling a carboxylic acid of Formula 2 with an aniline of Formula 3 in the presence of a coupling agent.
    Type: Application
    Filed: May 23, 2014
    Publication date: September 11, 2014
    Applicant: Vertex Pharmaceuticals Incorporated
    Inventors: John DeMattei, Adam R. Looker, Bobbianna Neubert-Langille, Martin Trudeau, Stefanie Roeper, Michael P. Ryan, Dahrika Milfred Yap Guerette, Brian R. Krueger, Peter D.J. Grootenhuis, Fredrick F. Van Goor, Martyn C. Botfield, Gregor Zlokarnik
  • Publication number: 20140243289
    Abstract: The present invention relates to prodrugs of modulators of ABC transporters, particularly, CFTR modulators, compositions thereof, and methods therewith. The present invention also relates to methods of treating ABC transporter mediated diseases using such modulators.
    Type: Application
    Filed: May 2, 2014
    Publication date: August 28, 2014
    Applicant: Vertex Pharmaceuticals Incorporated
    Inventors: Peter D.J. Grootenhuis, Sara Hadida Ruah, Jinglan Zhou, Anna Hazlewood, Hayley Binch
  • Publication number: 20140243348
    Abstract: Compositions and methods that are useful for the treatment of herpesvirus infection (including herpes simplex virii) are disclosed. Methods for identifying compounds useful for the treatment of herpesvirus infection are also disclosed.
    Type: Application
    Filed: January 22, 2014
    Publication date: August 28, 2014
    Applicant: PRESIDENT AND FELLOWS OF HARVARD COLLEGE
    Inventors: David M. Knipe, Kevin Bryant, David H. Dreyfus
  • Publication number: 20140242172
    Abstract: The present invention relates to solid state forms of N-[2,4-bis(1,1-dimethylethyl)-5-hydroxyphenyl]-1,4-dihydro-4-oxoquinoline-3-carboxamide (Compound 1), pharmaceutical compositions thereof and methods therewith.
    Type: Application
    Filed: May 8, 2014
    Publication date: August 28, 2014
    Applicant: Vertex Pharmaceuticals Incorporated
    Inventors: Patricia Hurter, William Rowe, Christopher R. Young, Adriana Costache, Patrick R. Connelly, Mariusz Krawiec, Yuchuan Gong, Yushi Feng, Martin Trudeau