Ring Oxygen In The Additional Hetero Ring Patents (Class 549/60)
  • Patent number: 10328027
    Abstract: A new scalable process to control the particle size and the particle size distribution, comprising 5 steps: (i) suspension preparation in a mixture of solvents in which the API and/or excipient is partially soluble in one of the solvents; (ii) particle size reduction of the suspension; (iii) aging; (iv) stopping the aging by solvent removal; and (v) optionally, a step of isolating the processed ingredients in the form of powder.
    Type: Grant
    Filed: January 27, 2015
    Date of Patent: June 25, 2019
    Assignee: Hovione International Ltd.
    Inventors: Eunice Costa, Marcio Temtem, Luis Sobral, Constanca Cacela, Peter Villax
  • Patent number: 10323025
    Abstract: The present invention relates to an improved crystallization procedure to obtain canagliflozin hemihydrate crystals having a narrow particle size distribution by removing a small part of the crystalline suspension in the crystallization vessel from said vessel and subjecting said part to particle size reduction of the formed crystals followed by heating and reintroducting said part of the crystalline suspension again in the crystallization vessel which is kept within a specific temperature range.
    Type: Grant
    Filed: December 20, 2016
    Date of Patent: June 18, 2019
    Assignee: Janssen Pharmaceutica NV
    Inventors: Ruben De Keyser, Stijn Laps, Thomas Joachim Landewald Rammeloo, Koen Johan Herman Weerts
  • Patent number: 10227356
    Abstract: Compounds that inhibit CNKSR1, pharmaceutical compositions including compounds that inhibit CNKSR1 and methods of treating disease or disorders that respond to CNKSR1 inhibition are described herein. Additionally, methods of identifying inhibitors of CNKSR1 are described.
    Type: Grant
    Filed: April 20, 2016
    Date of Patent: March 12, 2019
    Assignee: PHUSIS THERAPEUTICS, INC.
    Inventors: D. Lynn Kirkpatrick, Martin Indarte
  • Patent number: 10160861
    Abstract: The present invention describes novel 7-alkylamino-3-(thienyl) coumarin fluorescent dyes of formula (I) These dyes are water soluble, can be excited by the 405 nm excitation source and exhibit a large Stokes shift (?80 nm). Furthermore, the dyes possess a reactive group for the labeling of biomolecules or other analytes.
    Type: Grant
    Filed: March 14, 2017
    Date of Patent: December 25, 2018
    Assignee: CYANAGEN S.r.l.
    Inventors: Thomas Paul Jansen, Giacomo Rodeghiero, Dario Foglietta, Rossana Perciaccante, Leopoldo Della Ciana
  • Patent number: 9999613
    Abstract: The invention relates to the use of the compound of general formula 1 or its spatial isomers as an analgesic drug. The compounds have high activity, low toxicity, may be used in medicine.
    Type: Grant
    Filed: June 10, 2015
    Date of Patent: June 19, 2018
    Assignee: OBSHESTVO S OGRANICHENNOI OTVETSVENNOSTJU “LEOFORS”
    Inventors: Ekaterina Vladimirovna Khaid, Alla Viktorovna Pavlova, Oksana Stanislavovna Mikhal'Chenko, Dina Vladimirovna Korchagina, Tatiana Genrihovna Tolstikova, Konstantin Petrovich Volcho, Veniamin Abramovich Khazanov, Nariman Faridovich Salakhutdinov
  • Patent number: 9090595
    Abstract: Compositions and methods for treating glaucoma are provided. In particular hydrophilic ester prodrugs and their use to reduce central corneal thickening is provided.
    Type: Grant
    Filed: February 20, 2014
    Date of Patent: July 28, 2015
    Assignee: Allergan, Inc.
    Inventors: Robert M. Burk, Wha Bin Im
  • Patent number: 9056850
    Abstract: The present invention is directed to a novel process for the preparation of compounds having inhibitory activity against sodium-dependent glucose transporter (SGLT) being present in the intestine or kidney.
    Type: Grant
    Filed: October 14, 2009
    Date of Patent: June 16, 2015
    Assignees: Janssen Pharmaceutica N.V., Mitsubishi Tanabe Pharma Corporation
    Inventors: Walter Ferdinand Maria Filliers, Rudy Laurent Maria Broeckx, Patrick Hubert J. Nieste, Masanori Hatsuda, Masahiko Yoshinaga, Mitsuhiro Yada, Christopher Teleha
  • Patent number: 9045462
    Abstract: The present disclosure provides processes for the preparation of a compound of Formula I: which is useful as an antiviral agent. The disclosure also provides compounds that are synthetic intermediates to compounds of formula.
    Type: Grant
    Filed: May 6, 2014
    Date of Patent: June 2, 2015
    Assignee: Gilead Sciences, Inc.
    Inventors: Jared Wayne Evans, Shinji Fujimori, Grace M. Huynh, Qi Liu, Martin Gerald Teresk
  • Publication number: 20150133659
    Abstract: The present invention relates to millepachine ((E)-1-(5-methoxy-2,2-dimethyl-2H-chromen-8-yl)-3-(4-methoxyphenyl)prop-2-en-1-one) and its analogues. The present invention provides methods for preparing these compounds, pharmaceutical compositions including these compounds, and methods of treating diseases utilizing pharmaceutical compositions including these compounds.
    Type: Application
    Filed: May 25, 2012
    Publication date: May 14, 2015
    Applicant: Sichuan University
    Inventors: Lijuan Chen, Yuquan Wei
  • Patent number: 9024042
    Abstract: Compositions and methods for treating glaucoma are provided. In particular hydrophilic ester prodrugs and their use to reduce central corneal thickening is provided.
    Type: Grant
    Filed: August 23, 2013
    Date of Patent: May 5, 2015
    Assignee: Allergan, Inc.
    Inventors: Wha-Bin Im, Robert M. Burk
  • Publication number: 20150080349
    Abstract: The present invention provides compounds and methods for modulation of the quorum sensing of bacteria. In an embodiment, the compounds of the present invention are able to act as replacements for naturally occurring bacterial quorum sensing ligands in a ligand-protein binding system; that is, they imitate the effect of natural ligands and produce an agonistic effect. In another embodiment, the compounds of the present invention are able to act in a manner which disturbs or inhibits the naturally occurring ligand-protein binding system in quorum sensing bacteria; that is, they produce an antagonistic effect. The compounds of the present invention comprise N-acylated-homoserine lactones (AHLs) comprised of a wide range of acyl groups.
    Type: Application
    Filed: July 10, 2014
    Publication date: March 19, 2015
    Inventors: Helen E. BLACKWELL, Grant D. GESKE, Jennifer C. CAMPBELL
  • Publication number: 20150072969
    Abstract: The present invention relates to phenyl alkanoic acid derivatives (the compounds of Formula (I)); and their isotopic forms, stereoisomeric and tautomeric forms and mixtures thereof in all ratios, or pharmaceutically acceptable salts, pharmaceutically acceptable solvates, prodrugs, polymorphs, N-oxides, S-oxides or carboxylic acid isosteres thereof. The invention also relates to processes for the preparation of compounds of Formula (I) and pharmaceutical compositions comprising one or more of the compounds of Formula (I). The said compounds and the pharmaceutical composition function as GPR (G-protein coupled receptor) agonists, particularly as GPR40 agonists, and are useful in the treatment of diseases or conditions mediated by GPR40. The present invention further relates to a method of treatment of diseases or conditions mediated by GPR40 comprising administering to a subject in need thereof a therapeutically effective amount of the compounds of Formula (I).
    Type: Application
    Filed: February 27, 2013
    Publication date: March 12, 2015
    Applicant: PIRAMAL ENTERPRISES LIMITED
    Inventors: Sanjay Kumar, Rajiv Sharma, Vishal Ashok Mahajan, Sangameshwar Prabhakar Sawargave
  • Publication number: 20150065343
    Abstract: The present invention relates to acrylamide compounds which are useful for combating or controlling invertebrate pests, in particular arthropod pests and nematodes, and to a method for producing them. The invention also relates to a method for controlling invertebrate pests by using these compounds and to plant propagation material and to an agricultural and a veterinary composition comprising said compounds.
    Type: Application
    Filed: March 28, 2013
    Publication date: March 5, 2015
    Inventors: Pascal Bindschaedler, Wolfgang Von Deyn, Karsten Koerber, Florian Kaiser, Ralph Paulini, Deborah L. Culbertson, Paul Neese, Franz Josef Braun
  • Publication number: 20150065497
    Abstract: Compounds of the present invention and pharmaceutically acceptable compositions thereof, are useful as modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator (“CFTR”). The present invention also relates to methods of treating ABC transporter mediated diseases using compounds of the present invention.
    Type: Application
    Filed: August 5, 2014
    Publication date: March 5, 2015
    Inventors: Sara S. Hadida Ruah, Mark T. Miller, Brian Bear, Jason McCartney, Peter D.J. Grootenhuis
  • Publication number: 20150048284
    Abstract: Problem to Be Solved: to provide a chromophore having a far superior nonlinear optical activity to conventional chromophores and to provide a nonlinear optical element comprising said chromophore. Solution: a chromophore comprising a donor structure D, a ?-conjugated bridge structure B, and an acceptor structure A, the donor structure D comprising an aryl group substituted with a substituted oxy group; and a nonlinear optical element comprising said chromophore.
    Type: Application
    Filed: June 27, 2014
    Publication date: February 19, 2015
    Inventors: Akira OTOMO, Isao AOKI, Hideki MIKI, Hidehisa TAZAWA, Shiyoshi YOKOYAMA
  • Publication number: 20150051257
    Abstract: Sulphonamide derivatives of benzylamine of formula (I), wherein A represents phenyl unsubstituted or substituted; or 9- or 10-membered bicyclic group, linked to —(O)x—(CH2)y— through one of its aromatic carbon atoms, consisting of benzene ring fused with -membered heteroaromatic ring containing 1 or 2 heteroatoms independently selected from the group consisting of N and O, wherein such bicyclic group is unsubstituted or substituted or with 5- or 6-membered non-aromatic heterocyclic ring having 1 or 2 O atoms, wherein heterocyclic ring is unsubstituted or substituted with one or more C1-C3-alkyls; D represents a group selected from: phenyl unsubstituted or substituted; naphthyl unsubstituted or substituted; thiophene unsubstituted or substituted; bicyclic group consisting of imidazolering fused with 5-membered non-aromatic carbocyclic ring; bicyclic group consisting of benzene ring fused with 5-membered heteroaromatic ring, having 1 or 2 heteroatoms independently selected from the group consisting of N, O and
    Type: Application
    Filed: March 20, 2013
    Publication date: February 19, 2015
    Applicant: ADAMED SP. ZO.O
    Inventors: Marcin Kolaczkowski, Monika Marcinkowska, Adam Bucki, Tomasz Lysakowski, Maciej Pawlowski
  • Publication number: 20150031658
    Abstract: This invention relates generally to the discovery of a method of inhibiting, preventing or treating bacterial infections. The invention also relates to a method of inhibiting bacterial capsule biogenesis.
    Type: Application
    Filed: October 15, 2014
    Publication date: January 29, 2015
    Inventors: Patrick C. Seed, Carlos C. Goller, Apurba Dutta, Brooks Maki, Frank Schoenen, James Noah, Lucile White
  • Patent number: 8940911
    Abstract: A library of unnatural squarylated homoserine lactones (SHLs) and squarylated lactones that bear potential to modulate biofilm formation in Gram negative bacteria. At low concentrations (˜200 ?M), these small molecules inhibit biofilm formation of E. coli. Moreover, these compounds are not toxic up to 300 ?M and do not significantly attenuate E. coli growth. The SHLs have potential to disperse established biofilm and demonstrate an enhanced reduction (˜50%) of the maximum biofilm thickness by use of SHLs during biofilm growth.
    Type: Grant
    Filed: August 1, 2013
    Date of Patent: January 27, 2015
    Assignee: Syracuse University
    Inventors: Yan-Yeung Luk, Sri Kamesh Narasimhan, Eric Falcone
  • Publication number: 20150025068
    Abstract: A compound of formula (I), useful for the treatment of cancer, inflammation and inflammatory disorders, and a pharmaceutical composition containing the compound.
    Type: Application
    Filed: December 21, 2012
    Publication date: January 22, 2015
    Inventors: Jessica Martinsson, Katarina Faernegardh, Mattias Joensson, Rune Ringom
  • Patent number: 8937189
    Abstract: Novel 3,6-disubstituted pyrans, optionally with a further substituent at the 4-position, are monoamine reuptake inhibitors with activity profiles of antidepressants.
    Type: Grant
    Filed: August 26, 2013
    Date of Patent: January 20, 2015
    Assignee: Wayne State University
    Inventor: Aloke K. Dutta
  • Publication number: 20150018330
    Abstract: The invention provides novel antimicrobial chemical entities based on a nitrothiazolide backbone that exhibit antibacterial and antiparasitic action against a wide range of human pathogens. The new classes of compounds show extended action against Gram positive bacteria including MRSA drug resistant pathogens. In the Gram-positive organisms, they specifically target and functionally inhibit microbial attachment to surfaces and biofilm formation. In Gram-negative bacteria, including enteroaggregative E. coli strains, these compounds function as pilicides by inhibiting the assembly of pilin subunits into adhesive filaments. Several of these compounds show potent antimicrobial action against Gram positive bacteria, perhaps involving novel targets. Many of the benzothiophene derivatives exhibit antimicrobial activity in the low micrograms per ml range and in blocking biofilm formation in the nanomolar range; ranges considered are well within the range of utility as therapeutics.
    Type: Application
    Filed: July 30, 2014
    Publication date: January 15, 2015
    Applicant: UNIVERSITY OF VIRGINIA PATENT FOUNDATION
    Inventors: Paul S. Hoffman, Richard L. Guerrant, Timothy L. MacDonald, Thomas Eric Ballard, JR.
  • Publication number: 20150011512
    Abstract: The invention relates to novel compounds for use in the treatment or prophylaxis of cancers and other proliferative conditions that are for example characterized by cells that express cytochrome P450 1B1 (CYP1B1) and allelic variants thereof. The invention also provides pharmaceutical compositions comprising one or more such compounds for use in medical therapy, for example in the treatment of prophylaxis of cancers or other proliferative conditions, as well as methods for treating cancers or other conditions in human or non-human animal patients. The invention also provides methods for identifying novel compounds for use in the treatment of prophylaxis of cancers and other proliferative conditions that are for example characterized by cells that express CYP1 B1 and allelic variants thereof. The invention also provides a method for determining the efficacy of a compound of the invention in treating cancer.
    Type: Application
    Filed: September 12, 2014
    Publication date: January 8, 2015
    Inventors: Steven Albert Everett, Saraj Ulhaq
  • Patent number: 8927741
    Abstract: The present disclosure provides a processes for the preparation of a compound of Formula I: which is useful as an antiviral agent. The disclosure also provides compounds that are synthetic intermediates to compounds of Formula I.
    Type: Grant
    Filed: March 13, 2013
    Date of Patent: January 6, 2015
    Assignee: Gilead Sciences, Inc.
    Inventors: William John Watkins, Qi Liu
  • Publication number: 20140361266
    Abstract: A condensed cyclic compound of Formula 1 is provided. An organic light-emitting device includes the same.
    Type: Application
    Filed: February 14, 2014
    Publication date: December 11, 2014
    Applicant: Samsung Display Co., Ltd.
    Inventors: Hye-Jin Jung, Seok-Hwan Hwang, Young-Kook Kim, Jun-Ha Park, Eun-Young Lee, Jin-O Lim, Sang-Hyun Han, Eun-Jae Jeong, Soo-Yon Kim
  • Patent number: 8889732
    Abstract: Fused heterocyclic compounds useful for prevention, treatment or improvement of diseases against which activation of the thrombopoietin receptor is effective are provided. A compound represented by the formula (I) (wherein R1 is an aryl group fused to a saturated ring or the like, A, B, L1, R2, L2, L3, Y, L4, R3 and X are defined in the description), a tautomer, prodrug or a pharmaceutically acceptable salt of the compound or a solvate thereof.
    Type: Grant
    Filed: October 22, 2010
    Date of Patent: November 18, 2014
    Assignee: Nissan Chemical Industries, Ltd.
    Inventors: Yukihiro Shigeta, Shingo Umezawa, Shunsuke Iwamoto, Takanori Nakamura
  • Patent number: 8884030
    Abstract: Provided are compounds of Formula I: and pharmaceutically acceptable salts and esters thereof. The compounds, compositions, and methods provided are useful for the treatment of Flaviviridae virus infections, particularly hepatitis C infections.
    Type: Grant
    Filed: August 2, 2013
    Date of Patent: November 11, 2014
    Assignee: Gilead Sciences, Inc.
    Inventors: Eda Canales, Lee S. Chong, Michael O'Neil Hanrahan Clarke, Edward Doerffler, Scott E. Lazerwith, Willard Lew, Michael Mertzman, Philip A. Morganelli, William J. Watkins
  • Publication number: 20140329871
    Abstract: The present invention provides compounds having the general structural Formula (I): and pharmaceutically acceptable derivatives thereof, as described generally and in classes and subclasses herein, and additionally provides pharmaceutical compositions thereof, and methods for the use thereof for the treatment of any of a number of conditions or diseases involving fibrosis or dysproliferation.
    Type: Application
    Filed: December 2, 2012
    Publication date: November 6, 2014
    Applicant: ANGION BIOMEDICA CORP.
    Inventors: Rama K. Mishira, Bijoy Panicker, James G. Tarrant, Dong Sung Lim, Lambertus J.W.M. Oehlen, Dawoon Jung
  • Publication number: 20140323502
    Abstract: The invention is directed to a class of compounds, including the pharmaceutically acceptable salts of the compounds, having the structure of formula I: as defined in the specification. The invention is also directed to compositions containing and uses of the compounds of formula I.
    Type: Application
    Filed: February 13, 2014
    Publication date: October 30, 2014
    Inventors: Anton Franz Joseph Fliri, Randall James Gallaschun, Christopher John O'Donnell, Jacob Bradley Schwarz, Barbara Eileen Segelstein
  • Publication number: 20140323736
    Abstract: The present application relates to known and novel aryl- and hetarylcarboxamides of the formula (I) and to their use as medicaments for controlling endoparasites in animals or humans, and also to parasiticidal compositions, in particular endoparasites, comprising aryl- and hetarylcyclylcarboxamides.
    Type: Application
    Filed: November 23, 2012
    Publication date: October 30, 2014
    Inventors: Hans-Georg Schwarz, Axel Trautwein, Lothar Willms, Maike Hink, Peter Lummen, Ulrich Gorgens, Pierre-Yves Coqueron, Achim Harder, Claudia Welz
  • Patent number: 8865919
    Abstract: A sulfonium compound represented by formula (1), a photo-acid generator, and a method for producing a sulfonium compound are provided: wherein X represents an electron-donating group; R1 and R2 each represent an alkyl group, a cycloalkyl group, or the like; R3 and R4 each represent an arylene group or a heteroarylene group; R5 and R6 each represent an alkyl group, a cycloalkyl group, or the like; and A? and B? are anions that are different from each other. The sulfonium compound, when used as a photo-acid generator, can produce a uniform and excellent resist pattern.
    Type: Grant
    Filed: December 30, 2011
    Date of Patent: October 21, 2014
    Assignee: Korea Kumho Petrochemical Co., Ltd.
    Inventors: Hyun Sang Joo, Dong Chul Seo, Dae Kyung Yoon, Dae Hyeon Shin
  • Publication number: 20140309187
    Abstract: Crystalline solid forms and the amorphous form of the anti-HCV compound 5-(3,3-dimethylbutyn-1-yl)-3-[(cis-4-hydroxy-4-{[(3S)-tetrahydrofuran-3-yloxy]methyl}cyclohexyl){[(1R)-4-methylcyclohex-3-en-1-yl]carbonyl}amino]thiophene-2-carboxylic acid (Compound I) were prepared and characterized in the solid state: Also provided are processes of manufacture and methods of using the crystalline forms.
    Type: Application
    Filed: June 24, 2014
    Publication date: October 16, 2014
    Inventors: Ahmad Hashash, Scott Wolckenhauer, Bing Shi
  • Publication number: 20140303171
    Abstract: Compounds of Formula I are disclosed: wherein A, R1, R2, R3, R4A, R4B, R5, R6 and R7 are defined herein. The compounds encompassed by Formula I include compounds which are HIV protease inhibitors. The compounds and their pharmaceutically acceptable salts are useful for the prophylaxis or treatment of infection by HIV and the prophylaxis, treatment, or delay in the onset of AIDS. The compounds and their salts can be employed as ingredients in pharmaceutical compositions, optionally in combination with other antivirals, immunomodulators, antibiotics or vaccines.
    Type: Application
    Filed: October 26, 2012
    Publication date: October 9, 2014
    Inventors: Michael John Boyd, Jean-Francois Chiasson, Sheldon Crane, André Giroux
  • Patent number: 8853196
    Abstract: The present invention relates to aminochromane, aminothiochromane and amino-1,2,3,4-tetrahydroquinoline derivatives of the formula (I) or a physiologically tolerated salt thereof. The invention relates to pharmaceutical compositions comprising such aminochromane, aminothiochromane and amino-1,2,3,4-tetrahydroquinoline derivatives, and the use of such aminochromane, aminothiochromane and amino-1,2,3,4-tetrahydroquinoline derivatives for therapeutic purposes. The aminochromane, aminothiochromane and amino-1,2,3,4-tetrahydroquinoline derivatives are GlyT1 inhibitors.
    Type: Grant
    Filed: August 3, 2012
    Date of Patent: October 7, 2014
    Assignee: AbbVie Deutschland GmbH & Co. KG
    Inventors: Wilhelm Amberg, Udo Lange, Frauke Pohlki
  • Patent number: 8853679
    Abstract: A semiconducting compound comprising the structure: where R1 to R4 independently comprise, but are not limited to, optionally substituted straight, branched or cyclic alkyl chains having 2 to 20 (e.g. 2 to 12) carbon atoms, alkoxy, amino, amido, silyl, alkyl, alkenyl, aryl or hetero aryl; where X1 and X2 independently comprise S, O, NR5 or SiR6R7 where R8 to R7 independently comprise C1 to C5 branched, straight or cyclic alkyl chains; and where Ar1 comprises a heterocyclic ring, and where n is an integer between 1 and 4.
    Type: Grant
    Filed: August 5, 2010
    Date of Patent: October 7, 2014
    Assignee: Cambridge Display Technology Limited
    Inventors: Sheena Zuberi, Tania Zuberi
  • Publication number: 20140296531
    Abstract: Small molecule therapeutics for the treatment of parasitic diseases, in particular, semi-synthetic derivatives of the fugally-derived natural product merulin A for the treatment of African Sleeping Sickness.
    Type: Application
    Filed: July 28, 2012
    Publication date: October 2, 2014
    Applicant: THE REGENTS OF THE UNIVERSITY OF CALIFORNIA
    Inventors: Khanitha Pudhom, Gabriel Navarro, James McKerrow, Roger Linington
  • Publication number: 20140296254
    Abstract: Disubstituted 3,4-diamino-3-cyclobutene-1,2-dione compounds are described that correspond to general formula (I). Also described, are pharmaceutical compositions that include these compounds and methods of using these compounds and compositions for the treatment of chemokine-mediated diseases.
    Type: Application
    Filed: October 26, 2012
    Publication date: October 2, 2014
    Applicant: GALDERMA RESEARCH & DEVELOPMENT
    Inventors: Branislav Musicki, Jerôme Aubert, Jean-Guy Boiteaux, Laurence Clary, Patricia Rossio, Marlène Schuppli-Nollet
  • Patent number: 8846955
    Abstract: Problem to Be Solved: to provide a chromophore having a far superior nonlinear optical activity to conventional chromophores and to provide a nonlinear optical element comprising said chromophore. Solution: a chromophore comprising a donor structure D, a ?-conjugated bridge structure B, and an acceptor structure A, the donor structure D comprising an aryl group substituted with a substituted oxy group; and a nonlinear optical element comprising said chromophore.
    Type: Grant
    Filed: August 24, 2010
    Date of Patent: September 30, 2014
    Assignees: National Institute of Information and Communications Technology, Sumitomo Electric Industries, Ltd., Kyushu University, National University Corporation
    Inventors: Akira Otomo, Isao Aoki, Hideki Miki, Hidehisa Tazawa, Shiyoshi Yokoyama
  • Patent number: 8841340
    Abstract: Crystalline solid forms and the amorphous form of the anti-HCV compound 5-(3,3-dimethylbutyn-1-yl)-3-[(cis-4-hydroxy-4-{[(3S)-tetrahydrofuran-3-yloxy]methyl}cyclohexyl){[(1R)-4-methylcyclohex-3-en-1-yl]carbonyl}amino]thiophene-2-carboxylic acid (Compound I) were prepared and characterized in the solid state: Also provided are processes of manufacture and methods of using the crystalline forms.
    Type: Grant
    Filed: March 13, 2013
    Date of Patent: September 23, 2014
    Assignee: Gilead Sciences, Inc.
    Inventors: Ahmad Hashash, Scott Wolckenhauer, Bing Shi
  • Publication number: 20140275179
    Abstract: Disclosed are compounds, compositions and methods for treating of disorders that are affected by the modulation of the GPR120 receptor. Such compounds are represented by Formula (I) and Formula (II) as follows: wherein Y, R1, G, and Q are defined herein; and wherein R11, R21, R41, RB1 and G1, are defined herein.
    Type: Application
    Filed: March 7, 2014
    Publication date: September 18, 2014
    Applicant: Janssen Pharmaceutica NV
    Inventors: Zhihua Sui, Chaozhong Cai, Xuqing Zhang
  • Publication number: 20140275570
    Abstract: The present disclosure provides processes for the preparation of a compound of Formula I: which is useful as an antiviral agent. The disclosure also provides compounds that are synthetic intermediates to compounds of formula.
    Type: Application
    Filed: May 6, 2014
    Publication date: September 18, 2014
    Applicant: Gilead Sciences, Inc.
    Inventors: Jared Wayne Evans, Shinji Fujimori, Grace M. Huynh, Qi Liu, Martin Gerald Teresk
  • Publication number: 20140252278
    Abstract: Disclosed is a p-type organic semiconductive material that is easy to produce and that has a high planarity in its polymer skeleton, and also provides a photoelectric conversion material, a photoelectric conversion layer, a photoelectric conversion element, and an organic thin film solar cell each having high photoelectric conversion efficiency and using the p-type organic semiconductive material. Specifically, the invention provides a bibenzo[b]furan compound having at least one constitutional unit represented by the following formula (1) or (2), as well as a photoelectric conversion material, a photoelectric conversion layer, a photoelectric conversion element, and an organic thin film solar cell each using that compound for a p-type organic semiconductive material.
    Type: Application
    Filed: October 22, 2012
    Publication date: September 11, 2014
    Applicant: Adeka Corporation
    Inventors: Mineki Hasegawa, Toru Yano, Ryo Taniuchi
  • Publication number: 20140234238
    Abstract: The invention relates to specific benzodioxepin-3-one compounds, to a process for the preparation thereof and to the use thereof as dyes or as fluorescent emitters for organic electroluminescent devices (OLEDs) or for organic light-emitting electrochemical cells (OLECs), and to corresponding electronic devices.
    Type: Application
    Filed: September 17, 2012
    Publication date: August 21, 2014
    Applicant: MERCK PATENT GMBH
    Inventors: Thomas Rudolph, Philipp Buehle, Ralf Rosskopf
  • Publication number: 20140228416
    Abstract: This invention provides compounds of formula (I): wherein X1, X2, X3, R2, R4b, R1, 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: September 12, 2013
    Publication date: August 14, 2014
    Applicant: Millennium Pharmaceuticals, Inc.
    Inventors: Christopher Blackburn, Kenneth M. Gigstad, He Xu
  • Publication number: 20140221431
    Abstract: Disclosed in the present invention is a novel histone deacetylase inhibitor of benzamides and use thereof. The inhibitor has good efficacy in treating diseases caused by abnormal gene expression, such as tumours, endocrine disorders, immune system diseases, genetic diseases and nerve system diseases. The histone deacetylase inhibitor of benzamides is a compound of the following general chemical structural formula (I) or a salt thereof.
    Type: Application
    Filed: June 26, 2012
    Publication date: August 7, 2014
    Applicants: Shanghai Institute of Pharmaceutical Industry, Sinopharm A-think Pharmaceutical Co., Ltd
    Inventors: Jianqi Li, Qingwei Zhang, Zhidan Jia, Jiajing Wang
  • Publication number: 20140221351
    Abstract: The present invention relates to novel bis-sulfonamide derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of chemokine receptors.
    Type: Application
    Filed: April 8, 2014
    Publication date: August 7, 2014
    Applicant: ALLERGAN, INC.
    Inventors: HAIQING YUAN, RICHARD L. BEARD, XIAOXIA LIU, JOHN E. DONELLO, VEENA VISWANATH, MICHAEL E. GARST
  • Publication number: 20140206888
    Abstract: A method of preparing Compound (1): or a pharmaceutically acceptable salt thereof includes: a) reacting Compound (A) with 3,3-dimethylbut-1-yne in the presence of one or more palladium catalysts selected from the group consisting of Pd(PPh3)4 and Pd(PPh3)2Cl2, and one or more copper catalysts selected from the group consisting of CuI, CuBr, and CuCl, to generate Compound (B); b) treating Compound (B) with an acid to generate Compound (C): c) reducing the cyclohexanone of Compound (C) to cyclohexanol to generate Compound (D); and d) reacting Compound (D) with a base to generate Compound (1), wherein Compounds (A), (B), (C), and (D) are each as depicted herein.
    Type: Application
    Filed: January 24, 2014
    Publication date: July 24, 2014
    Applicant: Vertex Pharmaceuticals Incorporated
    Inventors: Valdas Jurkauskas, Piero L. Ruggiero, Stefanie Roeper, David Willcox, Michael Waldo, Dahrika Milfred Yap Guerette, Billie J. Kline, Hoa Q. Luong
  • Patent number: 8772512
    Abstract: The present invention relates to a crystallization procedure to obtain 1-(?-D-glucopyranosyl)-4-methyl-3-[5-(4-fluorophenyl)-2-thienylmethyl] benzene hemihydrate crystals having a narrow particle size distribution and improved flowability, bulk and tap density properties.
    Type: Grant
    Filed: July 8, 2010
    Date of Patent: July 8, 2014
    Assignee: Janssen Pharmaceutica NV
    Inventors: Thomas Joachim Landewald Rammeloo, Ruben De Keyser, Gustaaf Jozef Petrus Schildermans
  • Publication number: 20140186878
    Abstract: Compounds are provided that are either fluorogenic or fluorophoric. Compositions and articles that include the compounds are also provided. Additionally, methods of detecting a microorganism using the compounds are provided. The compounds are fluorinated and can be used advantageously under acidic conditions.
    Type: Application
    Filed: March 5, 2012
    Publication date: July 3, 2014
    Applicant: 3M INNOVATIVE PROPERTIES COMPANY
    Inventors: Stephen B. Roscoe, Shih-Hung Chou, Stephanie J. Moeller, Jesse D. Miller, Kurt J. Halverson, Jason W. Bjork
  • Publication number: 20140187467
    Abstract: A dioxirane-containing compound has a first substituent that is an alkyl, polyalkoxy, aryl, heteroaryl, or heterocyclyl group, and a second substituent that is an electron withdrawing group, and where the first and second substituents can optionally join to form a cycloalkyl or heterocyclyl group. The dioxirane-containing compound can be used as an oxidant, surfactant, and/or an ionic liquid.
    Type: Application
    Filed: July 20, 2012
    Publication date: July 3, 2014
    Inventor: Kraig ANDERSON
  • Patent number: 8759544
    Abstract: The present disclosure provides processes for the preparation of a compound of Formula I: which is useful as an antiviral agent. The disclosure also provides compounds that are synthetic intermediates to compounds of formula.
    Type: Grant
    Filed: March 13, 2013
    Date of Patent: June 24, 2014
    Assignee: Gilead Sciences, Inc.
    Inventors: Jared Wayne Evans, Shinji Fujimori, Grace M. Huynh, Qi Liu, Martin Gerald Teresk