Plural Ring Nitrogens In The Polycyclo Ring System Patents (Class 514/322)
  • Patent number: 8802664
    Abstract: The present patent application concerns new ligands of the H4-receptor of formula (I), their process of preparation and their therapeutic use.
    Type: Grant
    Filed: September 27, 2011
    Date of Patent: August 12, 2014
    Assignee: Bioproject
    Inventors: Isabelle Berrebi-Bertrand, Xavier Billot, Thierry Calmels, Marc Capet, Denis Danvy, Stephane Krief, Olivier Labeeuw, Jeanne-Marie Lecomte, Nicolas Levoin, Xavier Ligneau, Philippe Robert, Jean-Charles Schwartz
  • Patent number: 8802691
    Abstract: The invention relates to the use of domperidone or a pharmaceutically acceptable salt thereof at low doses to prevent and/or treat a disease associated with an alteration of the immune response such as Leishmaniosis.
    Type: Grant
    Filed: March 30, 2010
    Date of Patent: August 12, 2014
    Assignee: Laboratorios del Dr. Esteve, S.A.
    Inventors: David Sabate Elias, Josep M. Homedes Beguer, Pablo Gomez Ochoa
  • Publication number: 20140221369
    Abstract: The invention provides 5-deuterium enriched 2,4-thiazolidinediones and 2,4-oxazolidinediones, such as 5-(4-((6-(4-amino-3,5-dimethylphenoxy)-1-methyl-1H-benzo[d]imidazol-2-yl)methoxy)benzyl)-5-deutero-thiazolidine-2,4-dione, deuterated derivatives thereof, stereoisomers thereof, pharmaceutically acceptable salt forms thereof, and methods of treating medical disorders, such as cancer, using the same.
    Type: Application
    Filed: January 31, 2014
    Publication date: August 7, 2014
    Applicant: DEUTERX, LLC
    Inventor: Sheila DeWitt
  • Patent number: 8796253
    Abstract: This invention relates to novel heteroaryl substituted pyrazole compounds, pharmaceutical compositions containing such compounds and the use of those compounds or compositions for treating hyper-proliferative and/or angiogenesis disorders, as a sole agent or in combination with other active ingredients or therapeutic measures.
    Type: Grant
    Filed: May 8, 2008
    Date of Patent: August 5, 2014
    Assignee: Bayer Intellectual Property GmbH
    Inventors: Stephen Boyer, Michael Härter, Philip Wickens, Manoj Patel, Ellalahewage Sathyajith Kumarasinghe, Ajay Kumar Bhargava, Karl-Heinz Thierauch, Hartmut Beck, Susanne Greschat, Peter Ellinghaus, Patrick Paulus, Holger Hess-Stumpp
  • Patent number: 8796309
    Abstract: The present invention provides a pharmaceutical composition that can efficiently achieve its medicinal action by having excellent basic pharmacologically active substance absorbency, even the basic pharmacologically active substance is poorly soluble, the pharmaceutical composition being prepared by adding (i) a basic pharmacologically active substance together with (ii) a fatty acid and organic acid glycerol ester and/or fatty acid and organic acid polyglycerol ester.
    Type: Grant
    Filed: November 2, 2006
    Date of Patent: August 5, 2014
    Assignee: Otsuka Pharmaceutical Co., Ltd.
    Inventors: Yasuo Yamaguchi, Takakuni Matsuda, Yuso Tomohira
  • Patent number: 8796256
    Abstract: The present invention relates to compounds of Formula (I), methods for preparing these compounds, compositions, intermediates and derivatives thereof and for treating a condition including but not limited to ankylosing spondylitis, artherosclerosis, arthritis (such as rheumatoid arthritis, infectious arthritis, childhood arthritis, psoriatic arthritis, reactive arthritis), bone-related diseases (including those related to bone formation), breast cancer (including those unresponsive to anti-estrogen therapy), cardiovascular disorders, cartilage-related disease (such as cartilage injury/loss, cartilage degeneration, and those related to cartilage formation), chondrodysplasia, chondrosarcoma, chronic back injury, chronic bronchitis, chronic inflammatory airway disease, chronic obstructive pulmonary disease, diabetes, disorders of energy homeostasis, gout, pseudogout, lipid disorders, metabolic syndrome, multiple myeloma, obesity, osteoarthritis, osteogenesis imperfecta, osteolytic bone metastasis, osteomalac
    Type: Grant
    Filed: May 24, 2011
    Date of Patent: August 5, 2014
    Assignee: Janssen Pharmaceutica NV
    Inventors: Gilles Bignan, Wing Cheung, Micheal Gaul, Hui Huang, Xun Li, Raymond Patch, Sharmila Patel, Mark Player, Guozhang Xu, Bao-Ping Zhao, Jian Liu
  • Publication number: 20140205564
    Abstract: The present disclosure relates to compounds, compositions and methods for the treatment of hepatitis C virus (HCV) infection. Also disclosed are pharmaceutical compositions containing such compounds and methods for using these compounds in the treatment of HCV infection.
    Type: Application
    Filed: March 21, 2014
    Publication date: July 24, 2014
    Inventors: Jeffrey Lee Romine, Denis R. St. Laurent, Makonen Belema, Lawrence B. Snyder, Lawrence G. Hamann, John F. Kadow, Jayne Kapur, Andrew C. Good, Omar D. Lopez, Rico Lavoie, John A. Bender
  • Patent number: 8785449
    Abstract: Disclosed are carboxamide compounds, as well as pharmaceutical compositions and methods of use. One embodiment is a compound having the structure in which R1, R2, R3, R4, D, J, Z, T, p, q, w and x are as described herein. In certain embodiments, a compound disclosed herein activates the AMPK pathway, and can be used to treat metabolism-related disorders and conditions.
    Type: Grant
    Filed: September 18, 2012
    Date of Patent: July 22, 2014
    Assignee: Rigel Pharmaceuticals, Inc.
    Inventors: Jiaxin Yu, Hui Hong, Ihab S. Darwish, Xiang Xu, Rajinder Singh
  • Publication number: 20140200212
    Abstract: Substituted fused imidazole derivatives, methods of their preparation, pharmaceutical compositions comprising a substituted fused imidazole derivative, and methods of use in treating inflammation are provided. The substituted fused imidazole derivatives may control the activity or the amount or both the activity and the amount of heme-oxygenase.
    Type: Application
    Filed: March 17, 2014
    Publication date: July 17, 2014
    Applicant: High Point Pharmaceuticals, LLC
    Inventors: Adnan M.M. Mjalli, Dharma Rao Polisetti, Jareer Nabeel Kassis, Matthew J. Kostura, Mustafa Guzel, Otis Clinton Attucks, Robert Carl Andrews, Samuel Victory, Suparna Gupta
  • Publication number: 20140193363
    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.
    Type: Application
    Filed: January 15, 2014
    Publication date: July 10, 2014
    Applicant: ENANTA PHARMACEUTICALS, INC.
    Inventors: Yao-Ling Qiu, Ce Wang, Xiaowen Peng, Lu Ying, Yat Sun Or
  • Publication number: 20140187581
    Abstract: The present invention relates to novel compounds of formula (I), and their pharmaceutically acceptable salts and compositions containing them. The present invention also relates to a process for the preparation of above said novel compounds, and their pharmaceutically acceptable salts. The compounds of formula (I) are useful in the treatment of various disorders that are related to 5-HT4 receptors.
    Type: Application
    Filed: January 5, 2012
    Publication date: July 3, 2014
    Applicant: SUVEN LIFE SCIENCES LIMITED
    Inventors: Ramakrishna Nirogi, Abdul Rasheed Mohammed, Suresh Yarlagadda, Srinivasa Rao Ravella, Anil Karbhari Shinde, Ramasastri Kamphampati, Praveen Kumar Roayapalley, Pradeep Jayarajan, Gopinadh Bhyrapuneni, Sriramachandra Murthy Patnala, Jyothsna Ravula, Venkateswarlu Jasti
  • Publication number: 20140187535
    Abstract: The disclosure relates to Substituted Benzimidazole-Type Piperidine Compounds of Formula (I): and pharmaceutically acceptable salts or solvates thereof, e.g., a pharmaceutically acceptable salt or solvate, wherein R1, R2, R3, Qa, W, U, A, B, Z, a, and the dashed lines are as defined herein, compositions comprising an effective amount of a Substituted Benzimidazole-Type Piperidine Compound, and methods to treat or prevent a condition, such as pain, comprising administering to an animal in need thereof an effective amount of a Substituted Benzimidazole-Type Piperidine Compound.
    Type: Application
    Filed: December 23, 2013
    Publication date: July 3, 2014
    Applicants: Shionogi & Co., Ltd., Purdue Pharma L.P.
    Inventors: Nobuyuki TANAKA, Kenji YAMAWAKI, Jiangchao YAO, Jianming YU, Xiaoming ZHOU
  • Patent number: 8765786
    Abstract: A medicament for treating diseases associated with cholinergic properties in the central nervous system (CNS) and/or peripheral nervous system (PNS), diseases associated with smooth muscle contraction, endocrine disorders, neurodegenerative disorders and the like, which comprises a compound of Formula (I), wherein A is CR1E or a nitrogen atom, X—Y—Z is N—CO—NR3AR3B and the like, R1A to R1E are each independently a hydrogen atom and the like, R2A to R2D are each independently a hydrogen atom and the like, R3A and R3B are each independently an optionally-substituted C3-10 cycloalkyl and 15 the like, and n is 1 or 2 or a pharmaceutically acceptable salt thereof, which exhibits potent modulatory-effects on the activity of alpha-7 nicotinic acetylcholine receptor (alpha-7 nAChR).
    Type: Grant
    Filed: December 20, 2013
    Date of Patent: July 1, 2014
    Assignee: Dainippon Sumitomo Pharma Co., Ltd.
    Inventors: Shinya Usui, Hiroki Yamaguchi, Yoko Nakai
  • Publication number: 20140179709
    Abstract: This invention relates to compounds of formula I their salts, and pharmaceutically acceptable derivatives thereof, pharmaceutical compositions comprising these compounds and their use in the treatment of picornavirus infections in mammals, as well as novel intermediates useful in the preparation of the compounds of formula I.
    Type: Application
    Filed: December 20, 2013
    Publication date: June 26, 2014
    Applicant: Biota Scientific Management Pty Ltd
    Inventors: Keith Watson, Guy Krippner, Pauline Stanislawski, Darryl McConnell
  • Patent number: 8759345
    Abstract: The present invention is directed to benzoimidazole compounds of the formula (1) and enantiomers, diastereomers, racemates, and pharmaceutically acceptable salts thereof. Compounds of the present invention are useful in pharmaceutical compositions and methods for the treatment of disease states, disorders, and conditions modulated by prolyl hydroxylase activity.
    Type: Grant
    Filed: April 28, 2009
    Date of Patent: June 24, 2014
    Assignee: Janssen Pharmaceutica NV
    Inventors: Frances Meredith Hocutt, Barry Eastman Leonard, Jr., Hillary M Peltier, Victor K. Phuong, Michael H. Rabinowitz, Mark D Rosen, Kyle T. Tarantino, Hariharan Venkatesan, Lucy Xiumin Zhao
  • Publication number: 20140163055
    Abstract: Disclosed are methods of treating HIV infections comprising, in one aspect, administering compounds that are phospholipase D inhibitors. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.
    Type: Application
    Filed: December 11, 2013
    Publication date: June 12, 2014
    Inventors: H. Alex Brown, Craig W. Lindsley
  • Publication number: 20140163008
    Abstract: A dibenzoxepin derivative represented by the following general formula (I) wherein Y is a hydrogen atom and the like, RA is a hydrogen atom and the like, X is the formula (b3) wherein RB is a hydrogen atom and the like, and the like, A is the formula (a18) wherein R1 is a hydrogen atom and the like, and RC and RD are the same or different and each is a hydrogen atom and the like, and the like, which has a PPAR? agonist activity and the like, and useful as a therapeutic agent and/or prophylaxis agent and the like for type 2 diabetes and the like, or a pharmaceutically acceptable salt thereof and the like is provided.
    Type: Application
    Filed: August 3, 2011
    Publication date: June 12, 2014
    Applicant: KYOWA HAKKO KIRIN CO., LTD.
    Inventors: Keisuke Yamamoto, Tomohiro Tamura, Rina Nakamura, Kimihisa Ueno, Shintaro Hosoe
  • Publication number: 20140163002
    Abstract: The present invention provides compounds of Formula (Ia): or stereoisomers, tautomers, or pharmaceutically acceptable salts thereof, wherein all the variables are as defined herein. These compounds are selective factor XIa inhibitors or dual inhibitors of FXIa and plasma kallikrein. This invention also relates to pharmaceutical compositions comprising these compounds and methods of treating thromboembolic and/or inflammatory disorders using the same.
    Type: Application
    Filed: August 6, 2012
    Publication date: June 12, 2014
    Applicant: BRISTOL-MYERS SQUIBB COMPANY
    Inventors: Patrick Y.S. Lam, Charles G. Clark, James R. Corte, William R. Ewing, Paul J. Gilligan, Yoon Jeon, Wu Yang, Leon M. Smith, II, Yufeng Wang
  • Patent number: 8742116
    Abstract: The invention relates to 6-substituted isoquinolone derivatives of the formula (I) useful for the treatment and/or prevention of diseases associated with Rho-kinase and/or Rho-kinase mediated phosphorylation of myosin light chain phosphatase, and compositions containing such compounds.
    Type: Grant
    Filed: June 18, 2009
    Date of Patent: June 3, 2014
    Assignee: Sanofi
    Inventors: Oliver Plettenburg, Armin Hofmeister, Katrin Lorenz, Joachim Brendel, Matthias Löhn, John Weston
  • Patent number: 8741923
    Abstract: The invention provides compounds of Formula (I) for the treatment of multiple sclerosis and other diseases.
    Type: Grant
    Filed: December 15, 2009
    Date of Patent: June 3, 2014
    Assignee: Merck Serono SA
    Inventors: Mathilde Muzerelle, Anna Quattropani, Cyril Montagne, Jérôme Dorbais
  • Publication number: 20140148467
    Abstract: Disclosed are carboxamide compounds, as well as pharmaceutical compositions and methods of use. One embodiment is a compound having the structure in which R1, R2, R3, R4, D, J, Z, T, p, q, w and x are as described herein. In certain embodiments, a compound disclosed herein activates the AMPK pathway, and can be used to treat metabolism-related disorders and conditions.
    Type: Application
    Filed: February 3, 2014
    Publication date: May 29, 2014
    Applicant: Rigel Pharmaceuticals, Inc.
    Inventors: Jiaxin Yu, Hui Hong, Ihab S. Darwish, Xiang Xu, Rajinder Singh
  • Publication number: 20140135314
    Abstract: Piperidine compounds and pharmaceutically useful salts thereof, a pharmaceutical composition including an effective amount of the racemic or enantiomerically enriched piperidine compounds to treat gastrointestinal diseases, and a method of treating gastrointestinal diseases in a mammal are provided.
    Type: Application
    Filed: January 17, 2014
    Publication date: May 15, 2014
    Applicant: SK BIOPHARMACEUTICALS CO., LTD.
    Inventors: Coo-Min CHUNG, Hyung-Jin JUN, Jin-Sung KIM, Hui-Ho KIM, Hye-Kyung MIN, Yong-Gil KIM, Jong-Gil CHOI, Hongwook KIM
  • Publication number: 20140121195
    Abstract: Benzimidazole, benzopyrazole and benzotriazole compounds are provided which bind to CCR(4) and are useful for the treatment of diseases such as allergic diseases, autoimmune diseases, graft rejection and cancer.
    Type: Application
    Filed: October 17, 2013
    Publication date: May 1, 2014
    Applicant: ChemoCentryx, Inc.
    Inventors: Manmohan Reddy Leleti, Yandong Li, Venkat Reddy Mali, Jay Powers, Ju Yang
  • Publication number: 20140121243
    Abstract: A medicament for treating diseases associated with cholinergic properties in the central nervous system (CNS) and/or peripheral nervous system (PNS), diseases associated with smooth muscle contraction, endocrine disorders, neurodegenerative disorders and the like, which comprises a compound of Formula (I): wherein A is CR1E or a nitrogen atom, X—Y—Z is N—CO—NR3AR3B and the like, R1A to R1E are each independently a hydrogen atom and the like, R2A to R2D are each independently a hydrogen atom and the like, R3A and R3B are each independently an optionally-substituted C3-10 cycloalkyl and the like, and n is 1 or 2 or a pharmaceutically acceptable salt thereof, which exhibits potent modulatory-effects on the activity of ?7 nicotinic acetylcholine receptor (?7 nAChR).
    Type: Application
    Filed: December 20, 2013
    Publication date: May 1, 2014
    Inventors: Hiroki Yamaguchi, Shinya Usui, Yoko Nakai
  • Publication number: 20140121244
    Abstract: A medicament for treating diseases associated with cholinergic properties in the central nervous system (CNS) and/or peripheral nervous system (PNS), diseases associated with smooth muscle contraction, endocrine disorders, neurodegenerative disorders and the like, which comprises a compound of Formula (I): wherein A is CR1E or a nitrogen atom, X—Y—Z is N—CO—NR3AR3B and the like, R1A to R1E are each independently a hydrogen atom and the like, R2A to R2D are each independently a hydrogen atom and the like, R3A and R3B are each independently an optionally-substituted C3-10 cycloalkyl and the like, and n is 1 or 2 or a pharmaceutically acceptable salt thereof, which exhibits potent modulatory-effects on the activity of ?7 nicotinic acetylcholine receptor (?7 nAChR).
    Type: Application
    Filed: December 20, 2013
    Publication date: May 1, 2014
    Inventors: Hiroki Yamaguchi, Shinya Usui, Yoko Nakai
  • Patent number: 8703803
    Abstract: Provided are tris-quaternary ammonium compounds which are modulators of nicotinic acetylocholine receptors. Also provided are methods of using the compounds for modulating the function of a nicotinic acetylcholine receptor, and for the prevention and/or treatment of central nervous system disorders, substance use and/or abuse and or gastrointestinal tract disorders.
    Type: Grant
    Filed: September 21, 2012
    Date of Patent: April 22, 2014
    Inventors: Peter A. Crooks, Linda P. Dwoskin, Roger Papke, Guangrong Zheng, Sangeetha Sumithran
  • Publication number: 20140107151
    Abstract: The present disclosure provides compounds and pharmaceutically acceptable salts that are tyrosine kinase inhibitors, in particular BLK, BMX, EGFR, HER2, HER4, ITK, JAK3, TEC, BTK, and TXK and are therefore useful for the treatment of diseases treatable by inhibition of tyrosine kinases such as cancer and inflammatory diseases such as arthritis, and the like. Also provided are pharmaceutical compositions containing such compounds and pharmaceutically acceptable salts and processes for preparing such compounds and pharmaceutically acceptable salts.
    Type: Application
    Filed: May 16, 2012
    Publication date: April 17, 2014
    Applicant: Principia Biophama Inc.
    Inventors: David Michael Goldstein, Kenneth Albert Brameld
  • Publication number: 20140100230
    Abstract: Methods of treating a TRPC5 mediated disorder in a subject by administering an effective amount of a TRPC5 antagonist, such as a compound disclosed herein, are described.
    Type: Application
    Filed: December 10, 2013
    Publication date: April 10, 2014
    Applicant: HYDRA BIOSCIENCES, INC.
    Inventors: Jayhong A. Chong, Christopher Fanger, Magdalene M. Moran, Elisha Singer, Timothy Strassmaier, Howard Ng
  • Publication number: 20140094450
    Abstract: The present invention relates to benzoimidazole-carboxylic acid amide compounds of the formula I, in which R?, R?, R??, R1, R2, R3, R4, R5, R6 and Z are defined as indicated below. The compounds of the formula I are APJ receptor modulators, and are useful for the treatment of diseases associated with increased blood pressure for example. The invention furthermore relates to the use of compounds of the formula I, in particular as active ingredients in pharmaceuticals, and pharmaceutical compositions comprising them.
    Type: Application
    Filed: September 19, 2013
    Publication date: April 3, 2014
    Applicant: SANOFI
    Inventors: Stephanie HACHTEL, Paulus WOHLFART, John WESTON, Marco MUELLER, Elisabeth DEFOSSA, Katharina MERTSCH, Jian-Hui WENG, Robert Alan BINNIE, Farid ABDUL-LATIF, William Jerome BOCK, Armin WALSER
  • Patent number: 8686021
    Abstract: Use of a benzoyl derivative of 3-aminocarbazole to produce a drug for the preventive or therapeutic treatment of a disorder selected form the group comprising inflammatory processes, pain, fever, tumors, Alzheimer's disease and atherosclerosis. Method for the preventive or therapeutic treatment of a disorder selected from the group comprising inflammatory processes, pain, fever, tumors, Alzheimer's disease and atherosclerosis in which a therapeutically effective quantity of a benzoyl derivative of 3-aminocarbazole according to the invention is administered to an individual.
    Type: Grant
    Filed: May 3, 2006
    Date of Patent: April 1, 2014
    Assignee: Aziende Chimiche Riunite Angelini Francesco A.C.R.A.F. S.p.A.
    Inventors: Lorenzo Polenzani, Giorgina Mangano, Isabella Coletta, Maria Alessandra Alisi, Nicola Cazzolla, Guido Furlotti, Caterina Maugeri
  • Patent number: 8685451
    Abstract: This invention pertains to a multi-layered tablet for a triple combination release of active agents to an environment of use. More particularly, the invention pertains to a multi-layered tablet (1) comprising two external drug-containing layers (2 and 3) in stacked arrangement with respect to and on opposite sides of an oral dosage form (4) that provides a triple combination release of at least one active agent. In one embodiment of the invention the dosage form is an osmotic device. In another embodiment of the invention the dosage form is a gastro-resistant coated core. In yet another embodiment of the invention the dosage form is a matrix tablet. In a different embodiment the dosage form is a hard capsule.
    Type: Grant
    Filed: June 18, 2008
    Date of Patent: April 1, 2014
    Assignee: Osmotica Kereskedelmi és Szolgáltató KFT
    Inventors: Fernando G. Toneguzzo, Glenn A. Meyer, Marcelo A. Ricci, Marcelo A. Coppari, Ana C. Pastini, Gustavo A. Fischbein
  • Publication number: 20140088112
    Abstract: The present invention is directed to alkyne benzotriazole derivatives which are potentiators of metabotropic glutamate receptors, particularly the mGluR2 receptor, and which are useful in the treatment or prevention of neurological and psychiatric disorders associated with glutamate dysfunction and diseases in which metabotropic glutamate receptors are involved. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which metabotropic glutamate receptors are involved.
    Type: Application
    Filed: April 30, 2012
    Publication date: March 27, 2014
    Inventors: Scott D. Kuduk, Jason W. Skudlarek
  • Publication number: 20140088110
    Abstract: Compounds of formula (I) a tautomer or stereoisomer thereof, or a salt thereof, wherein ring B and the imidazole to which it is fused, R4, R6 and R7 have the meanings as given in the description and the claims, are effective inhibitors of the Pi3K/Akt pathway.
    Type: Application
    Filed: November 26, 2013
    Publication date: March 27, 2014
    Applicant: BAYER INTELLECTUAL PROPERTY GmbH
    Inventors: Swen HÖLDER, Armin ZÜLCH, Thomas BÄR, Thomas MAIER, Astrid ZIMMERMANN, Thomas BECKERS, Volker GEKELER, Hemant JOSHI, Yogesh MUNOT, Umesh BHISE, Sunil CHAVAN, Sachin SHIVATARE, Sarvesh PATEL, Vikas GORE
  • Publication number: 20140080828
    Abstract: This disclosure relates to antiviral compounds disclosed herein and uses related thereto. In certain embodiments, the disclosure relates to pharmaceutical compositions comprising 2-((benzo[d]imidazol-2-yl)thio)-N-phenylpropanamide derivatives, N-phenyl-2-((1-phenyl-benzo[d]imidazol-2-yl)thio)propanamide derivatives, or 2-((benzo[d]imidazol-2-yl)thio)-N-(2-chloro-4-methylphenyl)propanamide derivatives. The derivatives may be substituted with one or more substituents. Typically, the pharmaceutical composition comprises a compound of Formula (I), or salt, prodrug, or ester thereof wherein X, Y, and R1 to R7 are described herein.
    Type: Application
    Filed: March 28, 2012
    Publication date: March 20, 2014
    Applicants: CHILDREN'S HEATLHCARE OF ATLANTA, INC., EMORY UNIVERSITY
    Inventors: Richard K. Plemper, James P. Snyder, Aiming Sun, John M. Ndungu, Jeong-Joong Yoon
  • Publication number: 20140080869
    Abstract: Pan-genotypic HCV inhibitors are described. This invention also relates to methods of using these inhibitors to treat HCV infection.
    Type: Application
    Filed: September 17, 2013
    Publication date: March 20, 2014
    Applicant: ABBVIE INC.
    Inventors: Preethi KRISHNAN, Teresa (Iok-Chan) NG, Tami J. PILOT-MATIAS, Warren M. KATI, Clarence J. MARING, Neeta C. MISTRY, Thomas J. REISCH, Rolf WAGNER, Dachun LIU, John K. PRATT, Mark A. Matulenko, Ryan G. KEDDY
  • Publication number: 20140080807
    Abstract: The present invention relates to substituted indazole compounds which modulate the activity of protein kinases and are therefore useful in treating diseases caused by degulated protein kinase activity, like cancer. The present invention also provides methods for preparing these compounds, pharmaceutical compositions comprising these compounds, and methods of treating diseases utilizing such these compounds or the pharmaceutical compositions containing them.
    Type: Application
    Filed: May 7, 2012
    Publication date: March 20, 2014
    Applicant: NERVIANO MEDICAL SCIENCES S.R.L.
    Inventors: Andrea Lombardi Borgia, Marina Ciomei, Daniele Donati, Marcella Nesi
  • Publication number: 20140080868
    Abstract: Pan-genotypic HCV inhibitors are described. This invention also relates to methods of using these inhibitors to treat HCV infection.
    Type: Application
    Filed: September 17, 2013
    Publication date: March 20, 2014
    Applicant: ABBVIE INC.
    Inventors: Theresea (Iok-Chan) NG, Tami J. PILOT-MATIAS, Warren M. KATI, Preethi KRISHNAN, Clarence J. MARING, Neeta C. MISTRY, Thomas J. REISCH, Rolf WAGNER, Dachun LIU, John K. PRATT, Mark A. MATULENKO, Ryan G. KEDDY
  • Patent number: 8673893
    Abstract: Substituted indazole derivatives of formula (I) and pharmaceutically acceptable salts thereof, as defined in the specification, process for their preparation and pharmaceutical compositions comprising them are disclosed; the compounds of the invention may be useful in therapy in the treatment of diseases associated with a deregulated protein kinase activity, like cancer.
    Type: Grant
    Filed: September 12, 2012
    Date of Patent: March 18, 2014
    Assignee: Nerviano Medical Sciences S.r.l.
    Inventors: Andrea Lombardi Borgia, Maria Menichincheri, Paolo Orsini, Achille Panzeri, Ettore Perrone, Ermes Vanotti, Marcella Nesi, Chiara Marchionni
  • Patent number: 8674113
    Abstract: This invention relates to compounds of formula I their use as inhibitors of the microsomal prostaglandin E2 synthase-1 (mPGES-1), pharmaceutical compositions containing them, and their use as medicaments for the treatment and/or prevention of inflammatory diseases and associated conditions. A, L, M, W, R1, R2, R3, R4, R6, R7, R9, Ra, Rb have meanings given in the description.
    Type: Grant
    Filed: December 8, 2011
    Date of Patent: March 18, 2014
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Henning Priepke, Henri Doods, Alexander Heim-Riether, Raimund Kuelzer, Roland Pfau, Klaus Rudolf, Dirk Stenkamp
  • Patent number: 8669247
    Abstract: Provided herein are 2,5-disubstituted arylsulfonamides that are useful for modulating CCR3 activity, and pharmaceutical compositions thereof. Also provided herein are methods of their use for treating, preventing, or ameliorating one or more symptoms of a CCR3-mediated disorder, disease, or condition.
    Type: Grant
    Filed: March 18, 2013
    Date of Patent: March 11, 2014
    Assignee: Axikin Pharmaceuticals, Inc.
    Inventors: Tai Wei Ly, Marie Chantal Siu-Ying Tran, Erik Dean Raaum
  • Publication number: 20140066443
    Abstract: The present invention is directed to aminomethyl biaryl benzotriazole derivatives which are potentiators of metabotropic glutamate receptors, particularly the mGluR2 receptor, and which are useful in the treatment or prevention of neurological and psychiatric disorders associated with glutamate dysfunction and diseases in which metabotropic glutamate receptors are involved. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which metabotropic glutamate receptors are involved.
    Type: Application
    Filed: April 30, 2012
    Publication date: March 6, 2014
    Inventors: Douglas C. Beshore, Robert M. Garbaccio, Scott D. Kuduk, Adam W. Johnson, Jason W. Skudlarek
  • Publication number: 20140065095
    Abstract: The invention relates to novel pyrrolidine derivatives of formula (I): wherein R1, R2 and R3 are as defined herein, as inhibitors of glutaminyl cyclase (QC, EC 2.3.2.5). QC catalyzes the intramolecular cyclization of N-terminal glutamine residues into pyroglutamic acid (5-oxo-prolyl, pGlu*) under liberation of ammonia and the intramolecular cyclization of N-terminal glutamate residues into pyroglutamic acid under liberation of water.
    Type: Application
    Filed: June 5, 2013
    Publication date: March 6, 2014
    Inventors: Ulrich Heiser, Daniel Ramsbeck, Robert Sommer, Antje Meyer, Torsten Hoffmann, Livia Boehme, Hans-Ulrich Demuth
  • Publication number: 20140057942
    Abstract: The present invention relates to new kinase inhibitors of Formula (I), wherein X is oxygen, —NH—, or a direct bond; Y is —NH— or a direct bond; n is an integer from 0 to 4; m is an integer from 0 to 4; Cy represents a bivalent radical consisting of a satured (poly)cycle, including fused, bi-, spiro or bridged carbocycles and heterocycles; in particular selected from the group consisting of: Formula (II), Ar is selected from the group comprising: Formula (III), R2 is hydrogen or methyl; R8 is hydrogen, methyl, halogen, or alkynyl; R1 is an aryl or heteroaryl more specifically ROCK inhibitors, compositions, in particular pharmaceuticals, comprising such inhibitors, and to uses of such inhibitors in the treatment and prophylaxis of disease. In particular, the present invention relates to new ROCK inhibitors, compositions, in particular pharmaceuticals, comprising such inhibitors, and to uses of such inhibitors in the treatment and prophylaxis of disease.
    Type: Application
    Filed: April 27, 2012
    Publication date: February 27, 2014
    Applicant: AMAKEM NV
    Inventors: Dirk Leysen, Olivier Defert, Sandro Boland, Jo Alen, Arnaud Pierre Jean Bourin
  • Publication number: 20140057895
    Abstract: The present invention relates to a novel indazole- or pyrrolopyridine-derivative comprising a 5 membered heterocyclic substituent at 1 position thereof which has an agonistic action or a partial agonistic action against serotonin-4 receptor, and a pharmaceutical composition comprising the same.
    Type: Application
    Filed: June 6, 2012
    Publication date: February 27, 2014
    Inventors: Kazuhiro Mizuno, Junya Ikeda, Takanori Nakamura, Masato Iwata, Hiromichi Otaka, Nana Goto
  • Patent number: 8658639
    Abstract: The present invention provides a compound of formula (I): wherein R1a is optionally substituted C1-6 alkyl, etc.; R1m is hydrogen atom, etc.; G1, G2, G3 and G4 are (i), etc. ((i) G1 is —N(R1b)—, G2 is —CO—, G3 is —C(R1c)(R1d)—, and G4 is oxygen, etc.); R1b is optionally substituted C1-6 alkyl, etc.; R1c and R1d are each independently optionally substituted C1-6 alkyl, etc.; R2 is optionally substituted C1-6 alkyl, etc.; R3a, R3b, R3c and R3d are each independently a group: -A-B (A is a single bond, etc., B is hydrogen atom, etc.), etc.; n is 1, etc.; R5 is C1-4 alkoxycarbonyl, etc., or a pharmaceutically acceptable salt thereof, which is useful as a renin inhibitor.
    Type: Grant
    Filed: June 24, 2010
    Date of Patent: February 25, 2014
    Assignee: Dainippon Sumitomo Pharma Co., Ltd
    Inventors: Satoshi Suetsugu, Nobuhisa Fukuda, Yoshio Nakai, Takashi Takada, Yohei Ikuma, Hiroyuki Nakahira
  • Patent number: 8658635
    Abstract: The invention is directed to certain novel compounds of formula (I) and salts thereof. The compounds of the invention are inhibitors of PI3-kinase activity.
    Type: Grant
    Filed: June 3, 2009
    Date of Patent: February 25, 2014
    Assignee: GlaxoSmithKline Intellectual Property Development Limited
    Inventors: Ian Robert Baldwin, Kenneth David Down, Paul Faulder, Simon Gaines, Julie Nicole Hamblin, Joelle Le, Christopher James Lunniss, Nigel James Parr, Timothy John Ritchie, John Edward Robinson, Juliet Kay Simpson, Christian Alan Paul Smethurst
  • Publication number: 20140051679
    Abstract: The present teachings provide a compound represented by Structural Formula (I): or a pharmaceutically acceptable salt thereof. Also described are pharmaceutical compositions and methods of use thereof.
    Type: Application
    Filed: October 12, 2012
    Publication date: February 20, 2014
    Applicant: UNIVERISTY HEALTH NETWORKS
    Inventors: Heinz W. Pauls, Radoslaw Laufer, Yong Liu, Sze-Wan Li, Bryan T. Forrest, Yunhui Lang, Narendra Kumar B. Patel, Louise G. Edwards, Grace Ng, Peter B. Sampson, Miklos Feher, Donald E. Awrey
  • Publication number: 20140051700
    Abstract: Methods and compositions for agonizing a type-2 orexin receptor (OX2R) in a cell determined to be in need thereof, including the general method of (a) administering to a subject a cyclic guanidinyl OX2R agonist and (b) detecting a resultant enhanced wakefulness or increased resistance to diet-induced accumulation of body fat, or abbreviated recovery from general anesthesia or jet lag.
    Type: Application
    Filed: August 20, 2012
    Publication date: February 20, 2014
    Inventor: Masashi Yanagisawa
  • Publication number: 20140051688
    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 R1, R2, R3, Q, and G are defined herein.
    Type: Application
    Filed: August 16, 2013
    Publication date: February 20, 2014
    Applicant: Janssen Pharmaceutica NV
    Inventors: Michael WINTERS, Zhihua Sui
  • Publication number: 20140051660
    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 R1, R2, R3, Q, and G are defined herein.
    Type: Application
    Filed: August 16, 2013
    Publication date: February 20, 2014
    Applicant: Janssen Pharmaceutica NV
    Inventors: Michael WINTERS, Zhihua Sui, Christopher Flores