The Chalcogen, X, Is In A -c(=x)- Group Patents (Class 548/180)
  • Patent number: 9745275
    Abstract: Provided is a pain-related compound, a pain-related pharmaceutical composition, and use of the same. Provided in one or more embodiments is a compound represented by Formula (I), a prodrug of the same, or a pharmaceutically permissible salt of any of the same.
    Type: Grant
    Filed: December 18, 2014
    Date of Patent: August 29, 2017
    Assignees: KYOTO UNIVERSITY, KAGOSHIMA UNIVERSITY
    Inventors: Masatoshi Hagiwara, Masayasu Toyomoto, Takamitsu Hosoya, Suguru Yoshida, Takashi Kurihara
  • Publication number: 20150133495
    Abstract: Disclosed herein is a compound of Formula I or a pharmaceutically acceptable salt thereof, in which A, G, R1 and R2 are as defined herein. The compounds and pharmaceutical compositions of the compounds are suitable for the treatment of HCV infection in mammals and are also useful to modulate or inhibit NS3/4 dimerization.
    Type: Application
    Filed: November 13, 2014
    Publication date: May 14, 2015
    Inventor: Daniel Lamarre
  • Patent number: 9018206
    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: Grant
    Filed: September 12, 2012
    Date of Patent: April 28, 2015
    Assignees: AbbVie Deutschland GmbH & Co. KG, AbbVie Inc.
    Inventors: Helmut Mack, Andreas Kling, Katja Jantos, Achim Moeller, Wilfried Hornberger, Charles W. Hutchins
  • 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: 20150105403
    Abstract: Described herein are compounds that are estrogen receptor modulators. Also described are pharmaceutical compositions and medicaments that include the compounds described herein, as well as methods of using such estrogen receptor modulators, alone and in combination with other compounds, for treating diseases or conditions that are mediated or dependent upon estrogen receptors.
    Type: Application
    Filed: March 14, 2013
    Publication date: April 16, 2015
    Inventors: Nicholas D. Smith, Steven P. Govek, Mehmet Kahraman, Jackaline D. Julien, Johnny Y. Nagasawa, Karensa L. Douglas, Celine Bonnefous, Andiliy G. Lai
  • Patent number: 9006229
    Abstract: The invention provides compounds of formula I: or a salt thereof as described herein. The invention also provides pharmaceutical compositions comprising a compound of formula I, processes for preparing compounds of formula I, intermediates useful for preparing compounds of formula I and therapeutic methods for treating the proliferation of the HIV virus, treating AIDS or delaying the onset of AIDS or ARC symptoms in a mammal using compounds of formula I.
    Type: Grant
    Filed: April 20, 2012
    Date of Patent: April 14, 2015
    Assignee: Gilead Sciences, Inc.
    Inventors: Michael L. Mitchell, Paul A. Roethle, Lianhong Xu, Hong Yang, Ryan McFadden, Kerim Babaoglu
  • Publication number: 20150099260
    Abstract: A preservative for body fluids, proteins, cells and tissues comprising an effective amount of an AGE crosslink breaker for preventing formation of advanced glycation end products. The AGE crosslink breaker comprises a compound of Structure (1): wherein V, W, X, Y and Z are any atom suitable for a heterocyclic carbene or carbene precursor framework, including B, C, O, N, S, Se, P, and As in any chemically-feasible oxidation state; wherein Q, R, M, T and U are any atom or substituent, including but not limited to, H, CLn, NLn, PLn, OLn, SLn, SeLn, LnCl, LnBr, LnI, wherein L is any atom, substituent or group, and n is any integer such that Q, R, M, T, and U can access all chemically-feasible oxidation states; and wherein G comprises any charged counter ion including, but not limited to those derived from C, O, N, B, Al, S, Se, Cl, Br, I in any chemically-feasible oxidation state.
    Type: Application
    Filed: October 3, 2014
    Publication date: April 9, 2015
    Inventors: David Spiegel, Jeanne Hendrickson
  • Patent number: 8987314
    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: July 18, 2013
    Date of Patent: March 24, 2015
    Assignee: Bristol-Myers Squibb Company
    Inventors: Heather Finlay, Ji Jiang, Soong-Hoon Kim, Brandon Parkhurst, Jennifer X. Qiao, Tammy C. Wang, Zulan Pi, George O. Tora, John Lloyd, James A. Johnson
  • Patent number: 8957219
    Abstract: Disclosed is a compound which is useful as an endothelial lipase inhibitor.
    Type: Grant
    Filed: October 15, 2009
    Date of Patent: February 17, 2015
    Assignee: Shionogi & Co., Ltd.
    Inventors: Koji Masuda, Shiro Kida, Kyohei Hayashi, Manabu Katou, Naoki Yoshikawa, Akira Kugimiya, Mado Nakajima, Nobuyuki Tanaka
  • Publication number: 20150031694
    Abstract: The invention provides compounds of formula (I): wherein R1-R7 and W have any of the values defined in the specification, and salts thereof. The compounds have good solubility and are useful for treating bacterial infections.
    Type: Application
    Filed: March 21, 2013
    Publication date: January 29, 2015
    Inventors: Edmond J. LaVoie, Ajit Parhi, Yongzheng Zhang, Daniel S. Pilch, Malvika Kaul
  • Publication number: 20150018342
    Abstract: The present invention relates to fused pyrroledicarboxamides of the formula (I), in which R1 to R9, X, m and n are as defined in the claims. The compounds of the formula (I) are inhibitors of the acid-sensitive potassium channel TASK-1 and suitable for the treatment of TASK-1 channel-mediated diseases such as arrhythmias, in particular atrial arrhythmias like atrial fibrillation or atrial flutter, and respiratory disorders, in particular sleep-related respiratory disorders like sleep apnea, for example.
    Type: Application
    Filed: February 1, 2013
    Publication date: January 15, 2015
    Applicant: SANOFI
    Inventors: Laurent Bialy, Katrin Lorenz, Klaus Wirth, Klaus Steinmeyer, Gerhard Hessler
  • Patent number: 8921552
    Abstract: Compounds of general formula A useful as potential anticancer agents against human cancer cell lines and a process for the preparation thereof.
    Type: Grant
    Filed: August 2, 2013
    Date of Patent: December 30, 2014
    Assignee: Council of Scientific & Industrial Research
    Inventors: Ahmed Kamal, Adla Mallareddy, Paidakula Suresh, Rajesh V. C. R. N. C. Shetti, Harish Chandra Pal, Ajit Kumar Saxena
  • Patent number: 8912186
    Abstract: The invention provides specific small molecule compounds that allosterically regulate the activity or modulate protein-protein interactions of AGC protein kinases and the Aurora family of protein kinases, methods for their production, pharmaceutical compositions comprising same, and their use for preparing medicaments for the treatment and prevention of diseases related to abnormal activities of AGC protein kinases or of protein kinases of the Aurora family.
    Type: Grant
    Filed: October 16, 2009
    Date of Patent: December 16, 2014
    Assignee: Universitaet des Saarlandes
    Inventors: Matthias Engel, Wolfgang Fröhner, Adriane Stroba, Ricardo M. Biondi
  • Publication number: 20140364608
    Abstract: The present invention provides a pesticide comprising an aryloxyacetamide compound represented by formula (IV) (wherein in formula (IV), R1a represents an alkyl group or the like, R2 to R5 independently represents an alkyl group, X represents a halogen atom or the like, n represents an integer of 0 to 5, Z represents an oxygen atom or a sulfur atom) or salt thereof as an active ingredient.
    Type: Application
    Filed: February 12, 2013
    Publication date: December 11, 2014
    Applicant: Nippon Soda Co., Ltd.
    Inventors: Hironori Furukawa, Daisuke Hanai, Tetsuo Tamai, Yasuyuki Shiinoki
  • Patent number: 8883833
    Abstract: The invention relates to substituted benzothiazoles, benzoxazoles—and their counterparts having pyridine and pyrimidine rings replacing the benzene ring—that are PDE4 inhibitors useful for treating stroke, myocardial infarct, and cardiovascular inflammatory conditions, to pharmaceutical compositions comprising these compounds, and to methods for the treatment of stroke, myocardial infarct, and cardiovascular inflammatory conditions in a mammal. The compounds have general formula I: in which A and B are carbocycles or heterocycles.
    Type: Grant
    Filed: November 20, 2008
    Date of Patent: November 11, 2014
    Assignee: Decode Genetics EHF
    Inventors: Jasbir Singh, Mark E. Gurney, Alex Burgin, Vincent Sandanayaka, Alexander Kiselyov, Munagala Rao
  • Patent number: 8883437
    Abstract: The invention relates to the use of a compound having formula (I) as an enzymatic substrate for the detection of a nitroreductase activity, wherein: W1, W2, W3 and W4 are independently H, Br, Cl, F, I, alkyl, alkoxy, thiomethyl, perfluoroalkyl, nitro, cyano, carboxyl (including the esters or amides thereof) or any combination of same; n=0, 1 or 2; X is NR, CZ5Z6, S or O, R being H, alkyl, aralkyl, aryl, alkanoic or alkylsulphonic, Z5 and Z6 being an alkyl; Y is N or N+R, R being alkyl, aralkyl, aryl, alkanoic or alkylsulphonic; Z1, Z2, Z3 and Z4 are independently H, Br, Cl, F, I, alkyl, aryl, alkoxy, perfluoroalkyl, nitro, cyano, carboxyl, sulphonyl, including the sulphonyl or carboxyl amides or esters thereof, and the salts of same.
    Type: Grant
    Filed: July 29, 2010
    Date of Patent: November 11, 2014
    Assignee: bioMérieux S.A.
    Inventors: Olivier Fabrega, Arthur James, Sylvain Orenga, John Perry, Vindhya Salwatura, Stephen Stanforth
  • Publication number: 20140315945
    Abstract: The present invention relates to azole compounds. The present invention also relates to pharmaceutical compositions containing these compounds and methods of treating cancer by administering these compounds and pharmaceutical compositions to subjects in need thereof. The present invention also relates to the use of such compounds for research or other non-therapeutic purposes.
    Type: Application
    Filed: March 14, 2014
    Publication date: October 23, 2014
    Applicant: EPIZYME, INC.
    Inventors: John Emmerson Campbell, Kevin Wayne Kuntz
  • Patent number: 8865736
    Abstract: Compounds of formula (I) have antibacterial activity: wherein R represents hydrogen or 1, 2 or 3 optional substituents; W is ?C(R1)—; R1 is hydrogen and R2 is hydrogen, methyl, or fluorine; or R1 and R2 taken together are —CH2—, —CH2CH2, —O—, or, in either orientation, —O—CH2— or —OCH2CH2—; and R3 is a radical of formula -(Alk1)m-(Z)p-(Alk2)n-Q.
    Type: Grant
    Filed: November 28, 2011
    Date of Patent: October 21, 2014
    Assignee: Biota Scientific Pty Ltd
    Inventors: David Ryall Brown, Ian Collins, Lloyd George Czaplewski, David John Haydon
  • Publication number: 20140296223
    Abstract: This invention relates to a method for regulating skin pigmentation of a subject, comprising the step of administering the agent for inhibiting the expression or activation of Microphthalmia Transcription Factor (MITF) to the subject who is in need of regulation of skin pigmentation.
    Type: Application
    Filed: August 31, 2012
    Publication date: October 2, 2014
    Applicant: THE GENERAL HOSPITAL CORPORATION
    Inventors: David E. Fisher, Rizwan Haq, Hans Ragnar Valdemar Widlund
  • Publication number: 20140296524
    Abstract: Halo-organic heterocyclic compounds are described, in which at least two halogen atoms are bound to a nitrogen-containing heterocyclic terminal moiety of the compound, with at least one of such halogen atoms being iodine or bromine. Also described are polymethine dyes based on these heterocyclic compounds, and dendrimeric compounds and conjugates of such polymethine dyes. The polymethine dyes are characterized by enhanced properties, e.g., brightness, photostability, sensitivity and/or selective affinity that make them useful to target cancer cells, pathogenic microorganisms, and/or other biological materials, in applications such as photodynamic therapy, photodynamic antimicrobial chemotherapy (PACT), cancer treatment, selective removal or attachment of biological materials, antimicrobial coating materials, and other diagnostic, theranostic, spectrum shifting, deposition/growth, and analytic applications.
    Type: Application
    Filed: May 5, 2014
    Publication date: October 2, 2014
    Applicant: Nanoquantum Sciences, Inc.
    Inventors: Gary W. Jones, Anatoliy L. Tatarets, Leonid D. Patsenker
  • Publication number: 20140288302
    Abstract: A pharmaceutical composition including a compound of formula (I): its pharmaceutically acceptable salt, or a solvate thereof. Ring A is nitrogen-containing hetero ring, Ring A may be substituted with a substituent other than a group represented by formula: —C(R1R2)—C(?O)—NR3R4 and a group represented by formula: —R5, a broken line represents presence or absence of a bond, Z is —NR6—, ?N—, —O—, or —S—, R6 is halogen or substituted or unsubstituted alkyl, R1 and R2 are each independently hydrogen, halogen, hydroxy, cyano, nitro, carboxy or substituted or unsubstituted alkyl, R3 is hydrogen or substituted or unsubstituted alkyl, R4 is hydrogen or substituted or unsubstituted alkyl, R3 and R4 taken together with the adjacent nitrogen atom to which they are attached may form a substituted or unsubstituted ring, R5 is hydrogen, halogen, hydroxy, cyano, nitro, carboxy, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, or substituted or unsubstituted alkynyl.
    Type: Application
    Filed: March 18, 2014
    Publication date: September 25, 2014
    Applicant: Shionogi & Co., Ltd.
    Inventors: Koji MASUDA, Shiro KIDA, Kyohei HAYASHI, Manabu KATOU, Naoki YOSHIKAWA, Akira KUGIMIYA, Mado NAKAJIMA, Nobuyuki TANAKA
  • Publication number: 20140243282
    Abstract: The present invention relates to novel drug conjugates, where in two drugs are linked together through an appropriate linker having at least two functional groups capable of forming covalent bond with drugs D1 and D2. The invention also relates to developing novel compositions, methods for their preparation and their use in treating various disease conditions.
    Type: Application
    Filed: December 12, 2011
    Publication date: August 28, 2014
    Inventor: Satish Reddy Kallam
  • Publication number: 20140243338
    Abstract: The present invention provides compounds of Formula (I): or stereoisomers, tautomers, or pharmaceutically acceptable salts thereof, wherein all the variables are as defined herein. These compounds are selective ROCK inhibitors. This invention also relates to pharmaceutical compositions comprising these compounds and methods of treating cardiovascular, smooth muscle, oncologic, neuropathologic, autoimmune, fibrotic, and/or inflammatory disorders using the same.
    Type: Application
    Filed: February 28, 2014
    Publication date: August 28, 2014
    Inventors: Mimi L. Quan, Zilun Hu, Cailan Wang
  • Publication number: 20140221357
    Abstract: The present invention provides compounds of Formula (I) or Formula (III): [INSERT CHEMICAL STRUCTURE HERE] (I) [INSERT CHEMICAL STRUCTURE HERE] (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: September 25, 2012
    Publication date: August 7, 2014
    Applicant: Bristol-Myers Squibb Company
    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: 20140206095
    Abstract: Embodiments of probes for selectively detecting compounds having a thiol group and an amino group, e.g., cysteine and/or homocysteine, are disclosed, along with methods and kits for detecting the compounds in neutral media with the probes. The probes have a structure according to the general formula where R1-R4 independently are hydrogen hydroxyl, halogen, thiol, thioether, lower aliphatic, or lower alkoxy, x is an integer from 0 to 4, and each R5 independently is halogen, hydroxyl, thiol, thioether, lower aliphatic, or lower alkoxy. Embodiments of the disclosed probes are capable of undergoing condensation/cyclization reactions with cysteine and/or homocysteine. Cysteine and/or homocysteine can be selectively detected and identified by determining fluorescence emission of the probes at characteristic wavelengths.
    Type: Application
    Filed: August 2, 2012
    Publication date: July 24, 2014
    Applicant: State of Oregon Acting by and through the State Board of Higher Education on behalf of Portland st
    Inventors: Robert Strongin, Xiaofeng Yang
  • Publication number: 20140200215
    Abstract: Compounds, methods of making such compounds, pharmaceutical compositions and medicaments comprising such compounds, and methods of using such compounds to treat, prevent or diagnose diseases, disorders, or conditions associated with one or more of the lysophosphatidic acid receptors are provided.
    Type: Application
    Filed: March 12, 2013
    Publication date: July 17, 2014
    Inventors: Brad Owen Buckman, John Beamond Nicholas, Kumaraswamy Emayan, Scott D. Seiwert
  • Patent number: 8759533
    Abstract: Disclosed are compounds, compositions and methods for treating various diseases, syndromes, conditions and disorders, including pain. Such compounds are represented by Formula (I) as follows: wherein Q and Z are defined herein.
    Type: Grant
    Filed: March 13, 2013
    Date of Patent: June 24, 2014
    Assignee: Janssen Pharmaceutica NV
    Inventors: Peter J. Connolly, Mark J. Macielag, Bin Zhu
  • Patent number: 8759333
    Abstract: Disclosed are compounds, compositions and methods for treating various diseases, syndromes, conditions and disorders, including pain. Such compounds are represented by Formula (I) as follows: wherein Q and Z are defined herein.
    Type: Grant
    Filed: March 13, 2013
    Date of Patent: June 24, 2014
    Assignee: Janssen Pharmaceutica NV
    Inventors: Peter J. Connolly, Mark J. Macielag, Bin Zhu
  • Publication number: 20140148600
    Abstract: The present invention relates to thiazole compounds of formula I, the method for preparation and use thereof. More specifically, the present invention relates to novel derivatives of natural product largazole, the method for preparing them and their uses for treatments against tumor and multiple sclerosis as inhibitors of histone deacetylase.
    Type: Application
    Filed: May 7, 2012
    Publication date: May 29, 2014
    Inventors: Fajun Nan, Fei Chen, Yangming Zhang, Jia Li, Yubo Zhou, Mingbo Su, Jian DING, Linghua Meng, Xin Xie, Shixian Wang
  • Patent number: 8735323
    Abstract: The present invention relates N-5-membered, fused, heteroaryl-methylene-N-cycloalkyl-carboxamide derivatives, their thiocarboxamide or N-substituted carboximidamide analogues, all of formula (I) wherein A represents a carbo-linked 5-membered heterocyclyl group; T represents O, S, N—Rc, N—ORd, N—NRcRd or N—CN; Z1 to Z3; W1 to W5; Y1 to Y3 and p represent various substituents; their process of preparation; their use as fungicide active agents, particularly in the form of fungicide compositions and methods for the control of phytopathogenic fungi, notably of plants, using these compounds or compositions.
    Type: Grant
    Filed: July 31, 2008
    Date of Patent: May 27, 2014
    Assignee: Bayer Cropscience AG
    Inventors: Philippe Desbordes, Stéphanie Gary, Marie-Claire Grosjean-Cournoyer, Benoît Hartmann, Philippe Rinolfi, Arounarith Tuch, Jean-Pierre Vors
  • Patent number: 8703938
    Abstract: The present invention discloses compounds of Formula (I), or pharmaceutically acceptable salts, esters, or prodrugs thereof: which inhibit RNA-containing virus, particularly the hepatitis C virus (HCV). Consequently, the compounds of the present invention interfere with the life cycle of the hepatitis C virus and are also useful as antiviral agents. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from HCV infection. The invention also relates to methods of treating an HCV infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention. The present invention relates to novel antiviral compounds represented herein above, pharmaceutical compositions comprising such compounds, and methods for the treatment or prophylaxis of viral (particularly HCV) infection in a subject in need of such therapy with the compounds.
    Type: Grant
    Filed: September 10, 2010
    Date of Patent: April 22, 2014
    Assignee: Enanta Pharmaceuticals, Inc.
    Inventors: Yat Sun Or, Ce Wang, Lu Ying, Xiaowen Peng, Yao-Ling Qiu
  • Publication number: 20140100213
    Abstract: This invention relates to the use of triazolone derivatives for the modulation, notably the inhibition of the activity or function of fatty acid synthase (FAS). Suitably, the present invention relates to the use of triazolones in the treatment of cancer.
    Type: Application
    Filed: November 4, 2013
    Publication date: April 10, 2014
    Applicant: GlaxoSmithKline LLC
    Inventors: Nicholas David Adams, Christopher Joseph Aquino, Amita M. Chaudhari, Jonathan Michael Chergurovich, Terence John Kiesow, Cynthia Ann Parrish, Alexander Joseph Reif, Kenneth Wiggall
  • Patent number: 8691816
    Abstract: The present invention is directed to inhibitors of S-nitrosoglutathione reductase (GSNOR), pharmaceutical compositions comprising such GSNOR inhibitors, and methods of making and using the same.
    Type: Grant
    Filed: August 14, 2009
    Date of Patent: April 8, 2014
    Assignee: N30 Pharmaceuticals, Inc.
    Inventors: Jan Wasley, Gary J. Rosenthal, Xicheng Sun, Sarah Strong, Jian Qiu
  • Publication number: 20140066420
    Abstract: The present invention relates to wherein each symbol is as defined in the specification. The compound of the present invention has a superior RBP4-lowering action, and is useful as a medicament for the prophylaxis or treatment of disease and condition mediated by increased RBP4.
    Type: Application
    Filed: October 16, 2013
    Publication date: March 6, 2014
    Applicant: Takeda Pharmaceutical Company Limited
    Inventors: Shizuo KASAI, Tomohiro KAKU, Masahiro KAMAURA
  • Publication number: 20140051711
    Abstract: Described herein are compounds and pharmaceutical compositions containing such compounds, which modulate the activity of store-operated calcium (SOC) channels. Also described herein are methods of using such SOC channel modulators, alone and in combination with other compounds, for treating diseases or conditions that would benefit from inhibition of SOC channel activity.
    Type: Application
    Filed: October 14, 2013
    Publication date: February 20, 2014
    Applicant: CalciMedica Inc.
    Inventors: Jeffrey P. WHITTEN, Yazhong PEI, Jianguo CAO, Zhijun WANG, Evan ROGERS
  • Publication number: 20140045818
    Abstract: The invention provides compounds of formula I: or a salt thereof as described herein. The invention also provides pharmaceutical compositions comprising a compound of formula I, processes for preparing compounds of formula I, intermediates useful for preparing compounds of formula I and therapeutic methods for treating the proliferation of the HIV virus, treating AIDS or delaying the onset of AIDS or ARC symptoms in a mammal using compounds of formula I.
    Type: Application
    Filed: April 20, 2012
    Publication date: February 13, 2014
    Applicant: Gilead Sciences, Inc.
    Inventors: Michael L. Mitchell, Paul A. Roethle, Lianhong Xu, Hong Yang, Ryan McFadden, Kerim Babaoglu
  • Publication number: 20140039190
    Abstract: Compounds of general formula A useful as potential anticancer agents against human cancer cell lines and a process for the preparation thereof.
    Type: Application
    Filed: August 2, 2013
    Publication date: February 6, 2014
    Inventors: Ahmed Kamal, Adla Mallareddy, Paidakula Suresh, Rajesh V., C., R., N., C. Shetti, Harish Chandra Pal, Ajit Kumar Saxena
  • Publication number: 20140037564
    Abstract: Provided are a novel compound having skin-whitening, anti-oxidizing and PPAR activities and a medical use thereof, and the compound has skin-whitening activities for the suppression of tyrosinase, and accordingly, is useful for use in skin-whitening pharmaceutical composition or cosmetic products; has anti-oxidant activities, and accordingly, is useful for the prevention and treatment of skin-aging; and has PPAR activities, and in particular, PPAR? and PPAR? activities, and accordingly, is useful for use in pharmaceutical compositions or health foods which are effective for the prevention and treatment of obesity, metabolic disease, or cardiovascular disease.
    Type: Application
    Filed: February 8, 2012
    Publication date: February 6, 2014
    Applicant: Pusan National University Indusrtyuniversity
    Inventors: Hae Young Chung, Min Hi Park, Young Mi Ha, Yu Kyeong Han, Ji Young Park, Yun Jung Park, Jin Ah Kim, Ji Yeon Lee, Yu Min Song, Hyung Ryong Moon
  • Publication number: 20140031290
    Abstract: Compounds that bind the glucagon-like peptide 1 receptor (GLP-1) receptor are provided including compounds which are modulators of the GLP-1 receptors and compounds which are capable of inducing a stabilizing effect on the receptor for use in structural analyses of the GLP-1 receptor. Methods of synthesis, methods of therapeutic and/or prophylactic use, and methods of use in stabilizing GLP-1 receptor in vitro for crystallization of the GLP-1 receptor of such compounds are provided.
    Type: Application
    Filed: July 8, 2013
    Publication date: January 30, 2014
    Inventors: Marcus F. Boehm, Esther Martinborough, Manisha Moorjani, Liming Huang, Junko Tamiya, Mark T. Griffith, Thomas Fowler, Andrew Novak, Michael Knaggs, Premji Meghani
  • Patent number: 8586571
    Abstract: The present invention relates to wherein each symbol is as defined in the specification. The compound of the present invention has a superior RBP4-lowering action, and is useful as a medicament for the prophylaxis or treatment of disease and condition mediated by increased RBP4.
    Type: Grant
    Filed: October 17, 2008
    Date of Patent: November 19, 2013
    Assignee: Takeda Pharmaceutical Company Limited
    Inventors: Shizuo Kasai, Tomohiro Kaku, Masahiro Kamaura
  • Publication number: 20130296310
    Abstract: Compounds of the formula I: or a pharmaceutically acceptable salt thereof, wherein, R1 is a group of formula A or formula B, and X, R2, R3, R4, R5, R6, Ra and Rb are as defined herein. Also provided are methods of using the compounds for treating diseases mediated by a P2X3 and/or a P2X2/3 receptor antagonist and methods of making the subject compounds.
    Type: Application
    Filed: July 1, 2013
    Publication date: November 7, 2013
    Inventors: Li Chen, Michael Patrick Dillon, Lichun Feng, Ronald Charles Hawley, Minmin Yang
  • Publication number: 20130281433
    Abstract: Compounds disclosed herein including compounds of formula I?: and salts thereof are provided. Pharmaceutical compositions comprising compounds disclosed herein, processes for preparing compounds disclosed herein, intermediates useful for preparing compounds disclosed herein and therapeutic methods for treating an HIV infection using compounds disclosed herein are also provided.
    Type: Application
    Filed: April 19, 2013
    Publication date: October 24, 2013
    Inventors: Kerim Babaoglu, Gediminas Brizgys, Jake Cha, Xiaowu Chen, Hongyan Guo, Randall L. Halcomb, Xiaochun Han, Richard Huang, Hongtao Liu, Ryan McFadden, Michael L. Mitchell, Yingmei Qi, Paul A. Roethle, Lianhong Xu, Hong Yang
  • Patent number: 8552033
    Abstract: The invention relates to compounds of the formula I in which R1, R2, X, A, B and Y1 to Y4 have the meanings indicated in the claims, and/or a pharmaceutically acceptable salt and/or a prodrug thereof. Because of their properties as inhibitors of chemokine receptors, especially as CXCR2 inhibitors, the compounds of the formula I and the pharmaceutically acceptable salts and prodrugs thereof are suitable for the prevention and treatment of chemokine mediated diseases.
    Type: Grant
    Filed: December 17, 2008
    Date of Patent: October 8, 2013
    Assignee: SANOFI
    Inventors: Stephanie Hachtel, Juergen Dedio, Stephen Shimshock, Carolina Lanter
  • Publication number: 20130252842
    Abstract: Cyanine dye compounds having a substituted methine moiety that are nucleic acid stains, particularly for fluorescent staining of RNA, including compounds having the formula where R1 is a C1-C6 alkyl, sulfoalkyl, carboxyalkyl or C1-C6 alkoxy; each R2 is independently selected from the group consisting of H, C1-C6 alkyl, C1-C6 alkoxy, fused benzo, trifluoromethyl, amino, sulfo, carboxy and halogen, that is optionally further substituted; at least one of R3, R4, and R5 is an alkyl, aryl, heteroaryl, cyclic, or heterocyclic moiety that is optionally substituted by alkyl, amino, aminoalkyl, carboxy, nitro, or halogen; and the remaining R3, R4 or R5 are hydrogen; X is S, O, or Se; and D is a substituted or unsubstituted pyridinium, quinolinium or benzazolium moiety.
    Type: Application
    Filed: May 24, 2013
    Publication date: September 26, 2013
    Applicant: LIFE TECHNOLOGIES CORPORATION
    Inventors: Jason DALLWIG, David Hagen, Ching-Ying Cheung, Gerald Thomas, Stephen Yue
  • Publication number: 20130231604
    Abstract: Halo-organic heterocyclic compounds are described, in which at least two halogen atoms are bound to a nitrogen-containing heterocyclic terminal moiety of the compound, with at least one of such halogen atoms being iodine or bromine. Also described are polymethine dyes based on these heterocyclic compounds, and dendrimeric compounds and conjugates of such polymethine dyes. The polymethine dyes are characterized by enhanced properties, e.g., brightness, photostability, sensitivity and/or selective affinity that make them useful to target cancer cells, pathogenic microorganisms, and/or other biological materials, in applications such as photodynamic therapy, photodynamic antimicrobial chemotherapy (PACT), cancer treatment, selective removal or attachment of biological materials, antimicrobial coating materials, and other diagnostic, theranostic, spectrum shifting, deposition/growth, and analytic applications.
    Type: Application
    Filed: March 3, 2012
    Publication date: September 5, 2013
    Applicant: NANOQUANTUM SCIENCES, INC.
    Inventors: Gary W. Jones, Anatoliy L. Tatarets, Leonid D. Patsenker
  • Publication number: 20130217727
    Abstract: The present invention relates to fungicidal 1-(heterocyclic carbonyl)-2-substituted pyrrolidines and their thiocarbonyl derivatives, their process of preparation and intermediate compounds for their 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.
    Type: Application
    Filed: October 20, 2011
    Publication date: August 22, 2013
    Inventors: Jurgen Benting, Peter Dahmen, Philippe Desbordes, Stephanie Gary, Hiroyuki Hadano, Jean-Pierre Vors, Ulrike Wachendorff-Neumann
  • Patent number: 8501933
    Abstract: Compounds of the formula I: or a pharmaceutically acceptable salt thereof, wherein, R1 is a group of formula A or formula B, and X, R2, R3, R4, R5, R6, Ra and Rb are as defined herein. Also provided are methods of using the compounds for treating diseases mediated by a P2X3 and/or a P2X2/3 receptor antagonist and methods of making the subject compounds.
    Type: Grant
    Filed: July 26, 2010
    Date of Patent: August 6, 2013
    Assignee: Roche Palo Alto LLC
    Inventors: Li Chen, Michael Patrick Dillon, Lichun Feng, Ronald Charles Hawley, Minmin Yang
  • Publication number: 20130196968
    Abstract: Disclosed are compounds, compositions and methods for treating various diseases, syndromes, conditions and disorders, including pain. Such compounds are represented by Formula (I) as follows: wherein Q and Z are defined herein.
    Type: Application
    Filed: March 13, 2013
    Publication date: August 1, 2013
    Applicant: Janssen Pharmaceutica, NV
    Inventor: Janssen Pharmaceutica, NV
  • Patent number: 8481532
    Abstract: Vicinal substituted cyclopropyl compounds which are inhibitors of phosphodiesterase 10 are described as are processes, pharmaceutical compositions, pharmaceutical preparations and pharmaceutical use of the compounds in the treatment of mammals, including human(s) for central nervous system (CNS) disorders and other disorders which may affect CNS function, for example neurological, neurodegenerative and psychiatric disorders including, but not limited to, those comprising cognitive deficits or schizophrenic symptoms.
    Type: Grant
    Filed: July 9, 2009
    Date of Patent: July 9, 2013
    Assignee: EnVivo Pharmaceuticals, Inc.
    Inventors: Amy Ripka, Gideon Shapiro, Richard Chesworth
  • Publication number: 20130150367
    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: September 12, 2012
    Publication date: June 13, 2013
    Applicants: Abbott Laboratories, Abbott GmbH & Co. KG
    Inventors: Helmut Mack, Andreas Kling, Katja Jantos, Achim Moeller, Wilfried Hornberger, Charles W. Hutchins