Ring Chalcogen In The Bicyclo Ring System Patents (Class 514/260.1)
  • Publication number: 20130330322
    Abstract: A method of reducing the appearance of skin aging comprising the step of applying a topical composition to the skin of a human exhibiting one or more signs of skin aging selected from fine lines, wrinkles, decreased skin elasticity, decreased light reflection, uneven pigmentation (dyschromia), coarse texture, dryness, solar lentigos, seborrheic keratoses, decreased dermal thickness, and/or increased sebum production, wherein the composition consists essentially of a dermatologically acceptable carrier and a targeted immune response modifier selected the group consisting of: (i) a 5-amino thiazolo[4,5-d]pyrimidin-one compound; (ii) an 8-hydroxyadenine compound; (iii) an imidazo-1,5-napthyridine compound; (iv) a 2-substituted-8-oxodeazapurine; (v) methyl 2-(3-{[6-amino-2-butoxy-8-oxo-7H-purin-9(8H)-yl]methyl}phenyl)acetate; (vi) 2-(3-{[6-amino-2-butoxy-8-oxo-7H-purin-9(8H)-yl]methyl}phenyl)acetic acid; and (iii) methyl 2-(3-(((3-(6-amino-2-butoxy-8-oxo-7H-purin-9(8H)-yl)propyl)(3-(dimethylamino)propyl)amino) ph
    Type: Application
    Filed: August 14, 2013
    Publication date: December 12, 2013
    Applicant: Metabeauty, Inc.
    Inventor: Leslie Baumann
  • Patent number: 8604039
    Abstract: The invention relates to new dihydrothienopyrimidine of formula 1, as well as pharmacologically acceptable salts, diastereomers, enantiomers, racemates, hydrates or solvates thereof, wherein X is SO or SO2, but preferably SO, and wherein R1, R2 and R3 have the meanings given in the description, and which are suitable for the treatment of respiratory or gastrointestinal complaints or diseases, inflammatory diseases of the joints, skin or eyes, diseases of the peripheral or central nervous system or cancers, as well as pharmaceutical compositions which contain these compounds.
    Type: Grant
    Filed: January 4, 2012
    Date of Patent: December 10, 2013
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Pascale Pouzet, Christoph Hoenke, Rolf Goeggel, Birgit Jung, Peter Nickolaus, Dennis Fiegen, Thomas Fox
  • Patent number: 8598156
    Abstract: The invention is directed to substituted indoline derivatives. Specifically, the invention is directed to compounds according to Formula I: wherein R1, R2, and R3 are defined herein. The compounds of the invention are inhibitors of PERK and can be useful in the treatment of cancer, ocular diseases, and diseases associated with activated unfolded protein response pathways, such as Alzheimer's disease, stroke, Type 1 diabetes Parkinson disease, Huntington's disease, amyotrophic lateral sclerosis, myocardial infarction, cardiovascular disease, atherosclerosis, and arrhythmias, and more specifically cancers of the breast, colon, pancreatic, and lung. Accordingly, the invention is further directed to pharmaceutical compositions comprising a compound of the invention. The invention is still further directed to methods of inhibiting PERK activity and treatment of disorders associated therewith using a compound of the invention or a pharmaceutical composition comprising a compound of the invention.
    Type: Grant
    Filed: March 23, 2011
    Date of Patent: December 3, 2013
    Assignee: GlaxoSmithKline LLC
    Inventors: Jeffrey Michael Axten, Seth Wilson Grant, Dirk A. Heerding, Jesus Rual Medina, Stuart Paul Romeril, Jun Tang
  • Publication number: 20130317044
    Abstract: Carboxylic acid derivatives where R—R6, X, Y and Z have the meanings stated in the description, and the preparation thereof, are described. The novel compounds are suitable for controlling diseases.
    Type: Application
    Filed: November 27, 2012
    Publication date: November 28, 2013
    Applicant: Abbott Gmbh & Co. KG
    Inventor: Abbott Gmbh & Co. KG
  • Publication number: 20130317045
    Abstract: Provided herein are thienopyridine and thienopyrimidine compounds of formula (I) for treatment of JAK kinase mediated diseases, including JAK2 kinase-, JAK3 kinase- or TYK2 kinase-mediated diseases. Also provided are pharmaceutical compositions comprising the compounds and methods of using the compounds and compositions.
    Type: Application
    Filed: August 31, 2011
    Publication date: November 28, 2013
    Applicant: AMBIT BIOSCIENCES CORPORATION
    Inventors: Michael J. Hadd, Mark W. Holladay, Eduardo Setti
  • Patent number: 8586505
    Abstract: Novel 4-(3-butynyl)aminopyrimidine derivatives represented by general formula [I] are useful as pest control agents. In general formula [I], R1 is a mono- or bi-cyclic ring which may contain 0 to 3 heteroatoms, for example, phenyl or oxazolyl; R2 is a hydrogen atom, —R, —OR, —C(O)OR, —C(O)NHR, —CONR2 (wherein R is straight-chain or branched C1-8 alkyl, or the like), hydroxyalkyl, or the like; R3 is a hydrogen atom, a halogen atom, acyloxy represented by (straight-chain or branched C1-8 aliphatic hydrocarbon group) —CO—O—, or the like; and R4 is a hydrogen atom, a halogen atom, C1-6 alkyl, or the like, or alternatively, R4 and R3 together with the carbon atoms on the pyrimidine ring may form a thiophene ring, a pyrrole ring, an imidazole ring, a benzene ring, a pyrimidine ring, a furan ring, a pyrazine ring, or a pyrrolidine ring.
    Type: Grant
    Filed: July 15, 2010
    Date of Patent: November 19, 2013
    Assignee: SDS Biotech K. K.
    Inventors: Masaaki Sakai, Tomoaki Matsumura, Satohiro Midorikawa, Takashi Nomoto, Ryutaro Katsuki, Tomoko Muraki
  • Patent number: 8586580
    Abstract: Disclosed are a 2,7-substituted thieno[3,2-d]pyrimidine compound having a protein kinase inhibition activity, a pharmaceutically acceptable salt, and a pharmaceutical composition for prevention and treatment of diseases caused by abnormal cell growth comprising the compound as an effective ingredient. Since the novel 2,7-substituted thieno[3,2-d]pyrimidine compound exhibits superior inhibition activity against various protein kinases involved in growth factor signal transduction, it is useful as an agent for preventing or treating diseases caused by abnormal cell growth.
    Type: Grant
    Filed: October 15, 2010
    Date of Patent: November 19, 2013
    Assignee: Korea Institute of Science and Technology
    Inventors: Tae Bo Sim, Hwan Geun Choi, Jung Mi Hah, Young Jin Ham, Eun Jin Jun, Jung Hun Lee, Hwan Kim
  • Publication number: 20130303550
    Abstract: Compounds of formula (IIc); wherein X3 and X4 independently from each other are N or CR8 wherein R8 may be same or different; Y1, Y2, Y3 and Y4 independently from each other are N or CR9 wherein R9 may be same or different and wherein up to 3 of the group Y1, Y2, Y3 and Y4 may be N; their solvates, hydrates, and pharmaceutically acceptable salts, their use for modulating the Wnt signalling pathway activity and their use as a medicament, preferably for the treatment of cancer.
    Type: Application
    Filed: November 11, 2011
    Publication date: November 14, 2013
    Applicants: Ruprecht-Karls-Universitat Heidelberg, Deutsches Krebsforschungszentrum
    Inventors: Michael Boutros, Rajendra-Prasad Maskey, Corinna Koch, Florian Fuchs, Sandra Steinbrink, Daniel Gilbert
  • Publication number: 20130303533
    Abstract: Provided herein are azolopyridine and azolopyrimidine compounds for treatment of JAK kinase mediated diseases, including JAK2 kinase-, JAK3 kinase- or TYK2 kinase-mediated diseases. Also provided are pharmaceutical compositions comprising the compounds and methods of using the compounds and compositions.
    Type: Application
    Filed: August 31, 2011
    Publication date: November 14, 2013
    Applicant: AMBIT BIOSCIENCES CORPORATION
    Inventors: Qi Chao, Michael J. Hadd, Mark W. Holladay, Martin Rowbottom
  • Publication number: 20130303551
    Abstract: This invention relates to the use of pyrimidinone 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 pyrimidinones in the treatment of cancer.
    Type: Application
    Filed: January 10, 2012
    Publication date: November 14, 2013
    Inventors: Nicholas D. Adams, Alexander Joseph Reif, Kenneth Wiggall
  • Publication number: 20130296271
    Abstract: Agri-horticultural pest control compositions having outstanding control effect on pests, in particular, agri-horticultural pests, which comprise as active ingredients one or more 4-(3-butynyl)aminopyrimidine derivatives represented by the general formula [I], namely, where R1 is typically selected from among: a) phenyl c) —SiR5R6R7 (R5, R6, and R7 which may be the same or different represent a linear or branched alkyl having 1-6 carbon atoms, a linear or branched haloalkyl having 1-3 carbon atoms which is substituted by one halogen atom, a linear or branched cyanoalkyl having 1-3 carbon atoms which is substituted by one cyano group, and phenyl); d) hydropgen atom; R2 typically represents a hydrogen atom; R3 typically represents a hydrogen atom; R4 represents a hydrogen atom and one or more agri-horticultural pest control compounds selected from among agri-horticultural antimicrobial compounds, say, multi-site contact active compouns, nucleic acids synthesis inhibitory active compounds, mitosis and cell
    Type: Application
    Filed: December 27, 2011
    Publication date: November 7, 2013
    Applicant: SDS Biotech K.K.
    Inventors: Masaaki Sakai, Tomoaki Matsumura, Satohiro Midorikawa, Takashi Nomoto, Tomoko Muraki, Ryutaro Katsuki
  • Publication number: 20130296344
    Abstract: Compounds according to the general formula (I) wherein X1, X2, X3 and X4 independently from each other are N or CR8 wherein R8 may be same or different, and wherein up to 3 of the group X1, X2, X3 and X4 may be N; A is a 5- or 6-membered aromatic or heteroaromtic cycle containing 1 to 3 heteroatoms selected from the group consisting of N, O and S wherein A may be substituted by 1 to 5 substituents R which may be same or different; their solvates, hydrates, and pharmaceutically acceptable salts for the treatment of a disorder or disease associated with an aberrant activation of Wnt signalling in a mammal selected from a cell proliferative disorder, rheumatoid arthritis, increased bone density, aging or age-related disorders and/or diseases or Dupuytren disease (superficial fibromatosis).
    Type: Application
    Filed: November 11, 2011
    Publication date: November 7, 2013
    Applicants: Ruprecht-Karls-Universitat Heidelberg, Deutsches Krebsforschungszentrum
    Inventors: Michael Boutros, Rajendra-Prasad Maskey, Corinna Koch, Florian Fuchs, Sandra Steinbrink, Daniel Gilbert
  • Patent number: 8575178
    Abstract: The present invention is related to novel isothiazolo[3,4-d]pyrimidinedione and isothiazolo[5,4-d]pyrimidinedione derivatives as TRPA (Transient Receptor Potential subfamily A) modulators. In particular, compounds described herein are useful for treating or preventing diseases, conditions and/or disorders modulated by TRPA1 (Transient Receptor Potential subfamily A, member 1). Also provided herein are processes for preparing compounds described herein, intermediates used in their synthesis, pharmaceutical compositions thereof, and methods for treating or preventing diseases, conditions and/or disorders modulated by TRPA1.
    Type: Grant
    Filed: March 22, 2010
    Date of Patent: November 5, 2013
    Assignee: Glenmark Pharmaceuticals S.A.
    Inventors: Sukeerthi Kumar, Abraham Thomas, Sanjay Margal, Neelima Khairatkar-Joshi, Indranil Mukhopadhyay
  • Publication number: 20130289054
    Abstract: The present invention is related to novel thienopyrimidinedione derivatives as TRPA (Transient Receptor Potential subfamily A) modulators. In particular, compounds described herein are useful for treating or preventing diseases, conditions and/or disorders modulated by TRPA1 (Transient Receptor Potential subfamily A, member 1). Also provided herein are processes for preparing compounds described herein, intermediates used in their synthesis, pharmaceutical compositions thereof, and methods for treating or preventing diseases, conditions and/or disorders modulated by TRPA1.
    Type: Application
    Filed: June 25, 2013
    Publication date: October 31, 2013
    Inventors: Sukeerthi Kumar, Abraham Thomas, Nayan Taterao Waghmare, Sanjay Margal, Neelima Khairatkar-Joshi, Indranil Mukhopadhyay
  • Publication number: 20130287767
    Abstract: The invention discloses 4-(arylamino)selenophenopyrimidine derivatives of formula (I), hydrates, solvates, isomers, or pharmaceutically acceptable salts thereof; process for their preparation and methods of treating or inhibiting or controlling a cell proliferative disorders, particularly cancer using said compounds. Pharmaceutical compositions comprising 4-(arylamino)selenophenopyrimidine derivatives of formula (I) are useful for the treatment, inhibition, or control of cancer.
    Type: Application
    Filed: June 7, 2013
    Publication date: October 31, 2013
    Inventors: Ganga Raju GOKARAJU, Sudhakar KASINA, Venkateswarlu SOMEPALLI, Rama Raju GOKARAJU, Venkata Kanaka Ranga Raju GOKARAJU, Kiran BHUPHATIRAJU, Trimurtulu GOLAKOTI, Krishanu SENGUPTA, Venkata Krishna Raju ALLURI
  • Publication number: 20130281468
    Abstract: Bicyclic aryl substituted triazoles or heteroaryl substituted triazoles and pharmaceutical compositions containing the compounds are disclosed as being useful in inhibiting the activity of the receptor protein tyrosine kinase Axl. Methods of using the compounds in treating diseases or conditions associated with Axl activity are also disclosed.
    Type: Application
    Filed: June 14, 2013
    Publication date: October 24, 2013
    Inventors: Dane Goff, Jing Zhang, Rajinder Singh, Sacha Holland, Thilo J. Heckrodt, Pingyu Ding, Jiaxin Yu, Joane Litvak
  • Publication number: 20130281467
    Abstract: Compounds of formula (I), wherein G represents together with the two carbon atoms of the pyrimidine ring to which it is attached, a 5- to 7-membered aliphatic carbocyclic or heterocyclic ring system which contain 0 to 2 heteroatoms selected from the group consisting of nitrogen, oxygen and sulfur; and wherein said 5- to 7-membered aliphatic carbocyclic or heterocyclic ring system can be mono-, di- or trisubstituted by substituents selected from the group consisting of halogen, keto, C1-C6alkyl, C1-C6alkoxy, C1-C6alkyloximino and C1-C6alkylendioxy; and wherein the other substituents R1, R2, R3, R4, R5 and R6 are as defined in claim 1, and their use as microbicides.
    Type: Application
    Filed: October 28, 2011
    Publication date: October 24, 2013
    Applicant: SYNGENTA PARTICIPATIONS AG
    Inventors: Stephan Trah, Laura Quaranta, Clemens Lamberth, Martin Pouliot
  • Publication number: 20130274268
    Abstract: The present invention relates to a bicyclic compound for modulating G protein-coupled receptors. The inventive compound provides preventing or treating a disease associated with the modulation of G protein-coupled receptors, particularly GPR119 G protein-coupled receptors.
    Type: Application
    Filed: December 29, 2011
    Publication date: October 17, 2013
    Applicant: HANMI PHARM. CO., LTD
    Inventors: Jung Beom Son, Nam Du Kim, Young Kil Chang, Hee Cheol Kim, Ji Sook Kim, Young Hee Jung
  • Publication number: 20130274264
    Abstract: A method for treating diseases associated with the inhibition of phosphodiesterase 4 (PDE4) enzyme in a patient comprising administering to the patient in need thereof a therapeutically effective amount of a dihydrothienopyrimidinesulphoxide of formula 1, as well as pharmacologically acceptable salts, diastereomers, enantiomers, racemates, hydrates or solvates thereof
    Type: Application
    Filed: June 6, 2013
    Publication date: October 17, 2013
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: Pascale POUZET, Christoph HOENKE, Peter NICKOLAUS, Rolf GOEGGEL, Thomas FOX, Dennis FIEGEN, Klaus KLINDER
  • Publication number: 20130274101
    Abstract: The novel active compound combinations of a carboxamide of the general formula (I) (group 1) in which R, G, R1 and A have the meanings given in the description and the active compound groups (2) to (23) listed in the description have very good fungicidal properties.
    Type: Application
    Filed: June 12, 2013
    Publication date: October 17, 2013
    Inventors: Ulrike WACHENDORFF-NEUMANN, Peter Dahmen, Ralf Dunkel
  • Patent number: 8557866
    Abstract: The present invention relates to an isomeric composition comprising isomers of dinitro-octylphenyl esters, wherein the 2,6-dinitro-4-(1-propylpentyl)phenyl ester isomer is present in an amount of less than 0.1 weight percent, based on the total weight of the isomeric composition and to synergistic fungicidal mixtures therefrom.
    Type: Grant
    Filed: April 13, 2007
    Date of Patent: October 15, 2013
    Assignee: Dow AgroSciences, LLC.
    Inventors: Richard Billington, John Davies, Bernhard Distler, Robert J. Ehr, Franco Sivieri, Elizabeth Green, John T. Mathieson
  • Publication number: 20130266563
    Abstract: Selenophene compounds of formula (I) are described herein. In the compounds of Formula (I), ring A is a 6-membered aromatic fused ring, optionally containing one, two or three nitrogen atoms; a 5-membered heteroaromatic fused ring; or a mono- or bicyclic saturated heterocyclic fused ring having at least one ring member selected from the group consisting of N, O, S, SO and SO2; Y in ring B is nitrogen or substituted carbon; X is NR6, O, S, S(O), or S(O)2. R1, R2, R3, R4, and R6 are defined in the specification. Selenophene compounds of formula (I) may be used in methods of treating cell proliferative disorders, particularly cancer. Pharmaceutical compositions containing selenophene compounds of formula (I) may be used for treatment, inhibition, or control of cancer.
    Type: Application
    Filed: May 17, 2013
    Publication date: October 10, 2013
    Inventors: Ganga Raju Gokaraju, Sudhakar Kasina, Venkateswarlu Somepalli, Rama Raju Gokaraju, Venkata Kanaka Ranga Raju Gokaraju, Kiran Bhupathiraju, Trimurtulu Golakoti, Krishanu Sengupta, Venkata Krishna Raju Alluri
  • Patent number: 8551981
    Abstract: The present invention is directed to novel compounds of Formula (I) pharmaceutically acceptable salts, biologically active metabolites, pro-drugs, racemates, enantiomers, diastereomers, solvates and hydrates thereof wherein the variables are defined as herein. The compounds of Formula (I) are useful as kinase inhibitors and as such would be useful in treating certain conditions and diseases, especially inflammatory conditions and diseases and proliferative disorders and conditions, for example, cancers.
    Type: Grant
    Filed: October 7, 2011
    Date of Patent: October 8, 2013
    Assignee: AbbVie Inc.
    Inventors: David J. Calderwood, Noel S. Wilson, Philip Cox, Michael Z. Hoemann, Bruce Clapham, Anil Vasudevan, Clara I. Villamil, Bin Li, Gagandeep Somal, Kelly D. Mullen
  • Patent number: 8551965
    Abstract: A compound of formula (I) wherein Ar can be one six-membered or two fused six-membered aromatic rings; R8 and R9 can be hydrogen, alkyl, cycloalkyl, halogens, amino, alkylamino, dialkylamino, nitro, cyano, alkyoxy, aryloxy, thiol, alkylthiol, arythiol, or aryl; Q can be O, S or CY2, where Y may be H, alkyl or halogens; X can be O, NH, S, N-alkyl, (CHR2)m where m is 1 to 10, and CY2; Z can be O, S, NH, or N-alkyl; U? is H and U? can be H or CH2; wherein: T can be OH, H, halogens, O-alkyl, O-acyl, O-aryl, CN, NH2. or N3; T? and T? can be H or halogen; and W can be H or a phosphate group. Compounds show anti-viral activity, for example with respect to varicella zoster virus.
    Type: Grant
    Filed: September 24, 2010
    Date of Patent: October 8, 2013
    Assignees: University College Cardiff Consultants Limited, Rega Foundation
    Inventors: Christopher McGuigan, Jan Balzarini
  • Publication number: 20130261106
    Abstract: The present invention relates to compounds of formula (I): wherein R6 is —CONH2 or a —C(R?)(R?)(OH) group; R is a substituted phenyl or heteroaryl group; R7 is an optionally substituted aryl or heteroaryl group. Process for the preparation thereof and therapeutic use thereof.
    Type: Application
    Filed: April 2, 2013
    Publication date: October 3, 2013
    Applicant: SANOFI
    Inventors: Jean-Christophe CARRY, Fabienne CHATREAUX, Stephanie DEPRETS, Olivier DUCLOS, Vincent LEROY, Sergio MALLART, Dominique MELON-MANGUER, Maria MENDEZ-PEREZ, Fabrice VERGNE
  • Patent number: 8541421
    Abstract: The present invention provides, in part, substituted thieno[2,3-d]pyrimidines and methods of contacting compositions with such compounds to enhance the sweet taste of said compositions.
    Type: Grant
    Filed: March 18, 2011
    Date of Patent: September 24, 2013
    Assignee: Senomyx Inc.
    Inventors: Catherine Tachdjian, Xiao-Qing Tang, Sara Werner, Marketa Rinnova, Qing Chen, Guy Servant, Xiaodong Li, Feng Zhang, Haitian Liu, Albert Zlotnik, Mark Zoller, Boris Klebansky, Richard Fine, Xinshan Kang
  • Patent number: 8530652
    Abstract: Pyrrole pyrazole compounds of formula I, compositions including these compounds and methods of their use are provided. Preferred compounds of formula I have activity as protein kinase inhibitors, including as inhibitors of PAK4.
    Type: Grant
    Filed: October 6, 2011
    Date of Patent: September 10, 2013
    Assignees: Agouron Pharmaceuticals, Inc., Pfizer Inc.
    Inventors: Junhu Zhang, Chuangxing Guo, Djamal Bouzida, Liming Dong, Haitao Li, Joseph Timothy Marakovits, Anle Yang, Yufeng Hong
  • Patent number: 8530483
    Abstract: The present invention relates to novel amyloid binding compounds of formula (I) and methods for measuring effects of the compounds, by measuring changes of amyloid plaque level in living patients. More specifically, the present invention relates to a method of using the compounds of this invention as tracers in positron emission tomography (PET/) imaging to study amyloid deposits in brain in vivo to allow diagnosis of Alzheimer's disease. Thus, the present invention relates to use of the novel amyloid binding compounds as a diagnostic. The invention further relates to a method of measuring clinical efficacy of Alzheimer's disease therapeutic agents. Specifically, the present invention relates to novel aryl or heteroaryl substituted azabenzoxazole derivatives, compositions, and therapeutic uses and processes for making such compounds, or a pharmaceutically acceptable salt, solvate or in vivo hydrolysable ester thereof, wherein: X is O or S; A and Y independently are N, or CH.
    Type: Grant
    Filed: May 28, 2009
    Date of Patent: September 10, 2013
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: James C. Barrow, Scott Harrison, James Mulhearn, Cyrille Sur, David L. Williams, Scott Wolkenberg, Eric Hostetler
  • Patent number: 8524712
    Abstract: The present invention relates to compounds according to formulae (IA) to (ID) and compositions that inhibit the activity of Hsp90. The invention further relates to methods of inhibiting the activity of Hsp90 in a subject in need thereof and methods for preventing or treating hyperproliferative disorders, such as cancer, in a subject in need thereof comprising administering to the subject a compound of the invention, or a composition comprising such a compound.
    Type: Grant
    Filed: March 24, 2008
    Date of Patent: September 3, 2013
    Assignee: Synta Pharmaceuticals Corp.
    Inventors: Chi-Wan Lee, Teresa Przewloka, Weiwen Ying, Minghu Song, Zhenjian Du, Kevin Foley, Dan Zhou, Shuzhen Qin
  • Patent number: 8524719
    Abstract: This invention provides methods of inhibiting replication of a poxvirus by contacting a poxvirus with a compound having formula I, formula XXI, formula XXXII, or formula XLI which in turn reduce, inhibit, or abrogate poxvirus DNA polymerase activity and/or its interaction with its processivity factor. Formula I, formula XXI, formula XXXII, or formula XLI can be utilized to treat humans and animals suffering from a poxvirus infection. Pharmaceutical compositions for treating poxvirus infected subjects are also provided.
    Type: Grant
    Filed: August 21, 2012
    Date of Patent: September 3, 2013
    Assignee: The Trustees of the University of Pennsylvania
    Inventor: Robert P. Ricciardi
  • Publication number: 20130225609
    Abstract: The present invention relates to new medicament combinations which contain in addition to one or more PDE4-inhibitors (1) at least one EP4 receptor antagonist (2), as well as the use thereof for the treatment of preferably respiratory complaints such as particularly COPD, chronic sinusitis and asthma. The invention relates in particular to those medicament combinations which contain, in addition to one or more, preferably one, PDE4 inhibitor of general formula 1 wherein X is SO or SO2, but preferably SO, and wherein R1, R2, R3 and R4 have the meanings given in claim 1, at least one EP4 receptor antagonist (2), the preparation thereof and the use thereof for the treatment of respiratory complaints.
    Type: Application
    Filed: April 1, 2011
    Publication date: August 29, 2013
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventor: Peter Nickolaus
  • Patent number: 8507491
    Abstract: The invention provides a method, compounds and compositions for modulating the activity of the hedgehog signaling pathway. In particular, the invention provides a method for inhibiting aberrant growth states resulting from phenotypes such as Ptc loss-of-function, hedgehog gain-of-function, smoothened gain-of-function or GIi gain-of-function, comprising contacting a cell with a sufficient amount of a compound of Formula (I).
    Type: Grant
    Filed: August 24, 2009
    Date of Patent: August 13, 2013
    Assignee: IRM LLC
    Inventors: Dai Cheng, Dong Han, Guobao Zhang, Yongqin Wan, Yun Feng Xie, Jiqing Jiang, Wenqi Gao, Shifeng Pan
  • Patent number: 8507503
    Abstract: The present invention is related to novel thienopyrimidinedione derivatives as TRPA (Transient Receptor Potential subfamily A) modulators. In particular, compounds described herein are useful for treating or preventing diseases, conditions and/or disorders modulated by TRPA1 (Transient Receptor Potential subfamily A, member 1). Also provided herein are processes for preparing compounds described herein, intermediates used in their synthesis, pharmaceutical compositions thereof, and methods for treating or preventing diseases, conditions and/or disorders modulated by TRPA1.
    Type: Grant
    Filed: March 23, 2010
    Date of Patent: August 13, 2013
    Assignee: Glenmark Pharmaceuticals S.A.
    Inventors: Sukeerthi Kumar, Abraham Thomas, Nayan Taterao Waghmare, Sanjay Margal, Neelima Khairatkar-Joshi, Indranil Mukhopadhyay
  • Patent number: 8507502
    Abstract: Fused bicyclic or tricyclic compounds of formula (I): wherein A, B, C, X, Y, m, and n are defined herein. Also disclosed are a method for inhibiting EGFR kinase activity and a method for treating cancer with these compounds.
    Type: Grant
    Filed: November 9, 2009
    Date of Patent: August 13, 2013
    Assignee: National Health Research Institutes
    Inventors: Hsing-Pang Hsieh, Selvaraj Mohane Coumar, Tsu-An Hsu, Wen-Hsing Lin, Yi-Rong Chen, Yu-Sheng Chao
  • Patent number: 8501750
    Abstract: Heterocyclic compounds, pharmaceutical agent and methods thereof, having superior pharmacological action and/or physicochemical properties, which are useful for the prophylaxis or treatment of circulatory diseases such as hypertension, cardiac diseases, arteriosclerosis, renal diseases and cerebral apoplexy and/or metabolic diseases such as hyperlipidemia, obesity and diabetes and/or central nervous disorders such as cerebral infarction, and/or mental diseases such as dementia depression and depression.
    Type: Grant
    Filed: May 20, 2008
    Date of Patent: August 6, 2013
    Assignee: Takeda Pharmaceutical Company Limited
    Inventors: Takanobu Kuroita, Hideyuki Igawa, Hiroki Sakamoto, Kouhei Asano, Minoru Sasaki
  • Publication number: 20130196988
    Abstract: The present invention relates to dihydrothienopyrimidines, their use as modulators of ?-secretase and to pharmaceutical compositions containing said compounds. In particular, the present invention relates to compounds which interfere with ?-secretase and/or its substrate and therefore modulate the formation of A? peptides.
    Type: Application
    Filed: July 27, 2012
    Publication date: August 1, 2013
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: Kia GERLACH, Niklas HEINE, Scott HOBSON, Christoph HOENKE, Alexander WEBER
  • Publication number: 20130190297
    Abstract: The present invention relates to compound of Formula I, II, III, or IV, and/or a pharmaceutical acceptable addition salt thereof and/or a stereoisomer thereof and/or a solvate thereof, wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, R11, and R12 are as defined in the claim 1 or as described in detail in the description of the invention, and to the use of said compounds to treat or prevent viral infections and their use to manufacture a medicine to treat or prevent viral infections, particularly infections with RNA-viruses belonging to the family of the Retroviridae, the family of the Flaviviridae and the family of the Picornaviridae and more preferably infections with Human Immunodeficiency Virus 1 (HIV1), Human Immunodeficiency Virus 2 (HIV2), Hepatitis C virus (HCV), Dengue virus, and enteroviruses like Coxsackievirus, Rhinovirus and Poliovirus.
    Type: Application
    Filed: May 20, 2011
    Publication date: July 25, 2013
    Applicant: KATHOLIEKE UNIVERSITEIT LEUVEN, K.U.LEUVEN R&D
    Inventors: Steven De Jonghe, Ling-Jie Gao, Piet Herdewijn, Jean Herman, Miyeon Jang, Pieter Leyssen, Thierry Louat, Johan Neyts, Christophe Pannecouque, Bart Vanderhoydonck
  • Publication number: 20130183269
    Abstract: The present disclosure is generally directed to antiviral compounds, and more specifically directed to combinations of compounds which can inhibit the function of the NS5A protein encoded by Hepatitis C virus (HCV), compositions comprising such combinations, and methods for inhibiting the function of the NS5A protein.
    Type: Application
    Filed: January 7, 2013
    Publication date: July 18, 2013
    Applicant: Bristol-Myers Squibb Company
    Inventor: Bristol-Myers Squibb Company
  • Patent number: 8486952
    Abstract: The present disclosure provides a series of compounds of the formula (I) which modulate ?-amyloid peptide (?-AP) production and are useful in the treatment of Alzheimer's Disease and other conditions affected by ?-amyloid peptide (?-AP) production.
    Type: Grant
    Filed: July 28, 2010
    Date of Patent: July 16, 2013
    Assignee: Bristol-Myers Squibb Company
    Inventors: Kenneth M. Boy, Jason M. Guernon, John E. Macor, Richard E. Olson, Jianliang Shi, Lorin A. Thompson, III, Yong-Jin Wu, Li Xu, Yunhui Zhang, Dmitry S. Zuev
  • Patent number: 8486953
    Abstract: The present invention relates to novel pharmaceutical compositions comprising thienopyrimidine compounds. Moreover, the present invention relates to the use of the thienopyrimidine compounds of the invention for the production of pharmaceutical compositions for the prophylaxis and/or treatment of diseases which can be influenced by the inhibition of the kinase activity of Mnk1 and/or Mnk2 (Mnk2a or Mnk2b) and/or variants thereof.
    Type: Grant
    Filed: August 24, 2009
    Date of Patent: July 16, 2013
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Matthias Austen, Phillip Black, Wesley Blackaby, John Danilewicz, Ian Linney, Kay Schreiter, Martin Schneider
  • Publication number: 20130178462
    Abstract: The present disclosure provides a series of compounds of the formula (I) which modulate ?-amyloid peptide (?-AP) production and are useful in the treatment of Alzheimer's Disease and other conditions affected by ?-amyloid peptide (?-AP) production.
    Type: Application
    Filed: March 5, 2013
    Publication date: July 11, 2013
    Applicant: Bristol-Myers Squibb Company
    Inventor: Bristol-Myers Squibb Company
  • Publication number: 20130178460
    Abstract: The present invention relates to the use of novel compounds of Formula I: wherein all variable substituents are defined as described herein, which are SYK inhibitors and are useful for the treatment of auto-immune and inflammatory diseases.
    Type: Application
    Filed: January 10, 2013
    Publication date: July 11, 2013
    Applicant: Hoffmann-La Roche Inc.
    Inventor: Hoffmann-La Roche Inc.
  • Patent number: 8470850
    Abstract: The invention relates to the inhibition of VEGF receptor signaling and HGF receptor signaling. The invention provides compounds and methods for inhibiting VEGF receptor signaling and HGF receptor signaling.
    Type: Grant
    Filed: May 6, 2010
    Date of Patent: June 25, 2013
    Assignee: MethylGene Inc.
    Inventors: Arkadii Vaisburg, Stephen William Claridge, Franck Raeppel, Oscar Mario Saavedra, Noemy Berstein, Marie-Claude Granger, Lijie Zhan, Amal Wahhab, David Liewellyn
  • Publication number: 20130158051
    Abstract: The invention relates to oxazolopyrimidine compounds of formula (I), where A, R1, R2, R3, R4, X and Y are defined as stated in the claims. The compounds of formula I are suitable, for example, for wound healing.
    Type: Application
    Filed: January 12, 2011
    Publication date: June 20, 2013
    Applicant: SANOFI
    Inventors: Dieter Kadereit, Matthias Schaefer, Stephanie Hachtel, Axel Dietrich, Thomas Huebschle, Andreas Gille, Katrin Hiss
  • Patent number: 8466163
    Abstract: The present invention relates generally to chemical compounds and methods for their use and preparation. In particular, the invention relates to chemical compounds which may possess useful therapeutic activity, use of these compounds in methods of therapy and the manufacture of medicaments as well as compositions containing these compounds.
    Type: Grant
    Filed: December 11, 2007
    Date of Patent: June 18, 2013
    Assignee: Bionomics Limited
    Inventors: Bernard Luke Flynn, Jason Hugh Chaplin, Dharam Paul, Damian Wojciech Grobelny, Brian Kelly
  • Publication number: 20130137685
    Abstract: The invention relates to oxazolopyrimidine compounds of formula (I), where A, R1, R2 and R3 are defined as stated in the claims. The compounds of formula (I) are suitable, for example, for wound healing.
    Type: Application
    Filed: January 12, 2011
    Publication date: May 30, 2013
    Applicant: SANOFI
    Inventors: Dieter Kadereit, Matthias Schaefer, Stephanie Hachtel, Axel Dietrich, Thomas Huebschle, Andreas Gille, Katrin Hiss
  • Patent number: 8445491
    Abstract: The present invention generally relates to protein signalling. In particular, compounds that inhibit the Wnt protein signalling pathway are disclosed. Such compounds may be used in the treatment of Wnt protein signalling-related diseases and conditions such as cancer, degenerative diseases, type II diabetes and osteopetrosis.
    Type: Grant
    Filed: May 27, 2009
    Date of Patent: May 21, 2013
    Assignee: The Board of Regents of the University of Texas System
    Inventors: Lawrence Lum, Michael G. Roth, Baozhi Chen, Chuo Chen, Michael E. Dodge, Wei Tang
  • Publication number: 20130123279
    Abstract: Crystals are obtained by heating an aqueous suspension of 2-(3,4-dichlorobenzyl)-5-methyl-4-oxo-3,4-dihydrothieno[2,3-d]pyrimidine-6-carboxylic acid. Novel crystals are obtained by adjusting the heating temperature and/or duration.
    Type: Application
    Filed: May 31, 2011
    Publication date: May 16, 2013
    Applicant: ASKA PHARMACEUTICAL CO., LTD.
    Inventors: Hiroyuki Hayashi, Takayoshi Nakagawa, Koichi Miyazaki
  • Publication number: 20130123241
    Abstract: The present invention relates to novel antagonists for CCR2 (CC chemokine receptor 2) of formula (I) wherein HET is a group selected from among formulas (IIa) (IIb) (IIc) (IId) and their use for providing medicaments for treating conditions and diseases, especially pulmonary diseases like asthma and COPD and pain diseases.
    Type: Application
    Filed: May 10, 2011
    Publication date: May 16, 2013
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: Heiner Ebel, Sara Frattini, Riccardo Giovannini, Christoph Hoenke, Rocco Mazzaferro, Stefan Scheuerer
  • Publication number: 20130123231
    Abstract: The present invention provides compounds useful as inhibitors of Acetyl CoA Carboxylase (ACC), compositions thereof, and methods of using the same.
    Type: Application
    Filed: November 9, 2012
    Publication date: May 16, 2013
    Applicant: Nimbus Apollo, Inc.
    Inventor: Nimbus Apollo, Inc.