Bicyclo Ring Having The Additional Six-membered Nitrogen Hetero Ring As One Of The Cyclos Patents (Class 514/253.04)
Isoquinolines (including hydrogenated) (Class 514/253.05)
Quinolines (including hydrogenated) (Class 514/253.06)
  • Bicyclic aryl and bicyclic heteroaryl substituted triazoles useful as Axl inhibitors
    Patent number: 8492373
    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: Grant
    Filed: December 1, 2010
    Date of Patent: July 23, 2013
    Assignee: Rigel Pharmaceuticals, Inc.
    Inventors: Dane Goff, Jing Zhang, Rajinder Singh, Sacha Holland, Thilo J. Heckrodt, Pingyu Ding, Jiaxin Yu, Joane Litvak
  • HETERO RING-FUSED IMIDAZOLE DERIVATIVE HAVING AMPK ACTIVATING EFFECT
    Publication number: 20130184240
    Abstract: Disclosed is a compound which is useful as an AMPK activator. A compound represented by the formula: its pharmaceutically acceptable salt, or a solvate thereof, wherein a group represented by the formula: is a group represented by the formula: R1 is each independently halogen, hydroxy, cyano, nitro, carboxy, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl or the like; m is an integer of 0 to 3; R2 is hydrogen, or substituted or unsubstituted alkyl; X is —O—; and Y is substituted or unsubstituted aryl, or substituted or unsubstituted heteroaryl.
    Type: Application
    Filed: September 8, 2011
    Publication date: July 18, 2013
    Applicant: Shionogi & Co., Ltd.
    Inventors: Keisuke Tonogaki, Akira Ino, Eiichi Kojima, Manabu Katou, Masafumi Iwatsu, Nobuyuki Tanaka, Masahiko Fujioka
  • 3-(IMIDAZOLYL)-PYRAZOLO[3,4-B]PYRIDINES
    Publication number: 20130184289
    Abstract: Compounds are provided that act as potent antagonists of the CCR1 receptor, and have in vivo anti-inflammatory activity. The compounds are 3-imidazoyl-pyrazolo[3,4-b]pyridine derivatives and are useful in pharmaceutical compositions, methods for the treatment of CCR1-mediated disease, and as controls in assays for the identification of competitive CCR1 antagonists.
    Type: Application
    Filed: January 4, 2013
    Publication date: July 18, 2013
    Applicant: ChemoCentryx Inc.
    Inventor: ChemoCentryx Inc.
  • Antagonist of smoothened
    Patent number: 8486936
    Abstract: Described herein are compounds, pharmaceutical compositions and methods for the inhibition of Hedgehog signaling. Said compounds, pharmaceutical compositions and methods have utility in the treatment of human and veterinary diseases and disorders.
    Type: Grant
    Filed: May 4, 2010
    Date of Patent: July 16, 2013
    Assignee: AllaChem, LLC
    Inventors: Alexander Khvat, Sergey Tkachenko, Ilya Okun, Borys Rogovoy, Nikolay Savchuk, John May, Patrick O'Connor, William Ripka, Jean-Michel Vernier, David Matthews
  • Antifungal agents
    Patent number: 8486962
    Abstract: Compounds of formula (I), and pharmaceutically acceptable salts thereof, may be used in therapy, for example as antifungal agents: (I) wherein: R1, R2, R3, R4, R5, R6, R7, X and X1 are as defined herein. Certain compounds of formula (I) are also provided. Compounds of formula (T), and agriculturally acceptable salts thereof, may also be used as agricultural fungicides.
    Type: Grant
    Filed: May 18, 2006
    Date of Patent: July 16, 2013
    Assignee: F2G Ltd.
    Inventors: Samantha Patricia Thomson, Rhian Teresa Davies, Nigel Mark Allanson, Alexandre Kuvshinov, Gareth Morse Davies, Philip Neil Edwards
  • 3-(imidazolyl)-pyrazolo[3,4-b] pyridines
    Patent number: 8481545
    Abstract: Compounds are provided that act as potent antagonists of the CCR1 receptor, and have in vivo anti-inflammatory activity. The compounds are 3-imidazoyl-pyrazolo[3,4-b]pyridine derivatives and are useful in pharmaceutical compositions, methods for the treatment of CCR1-mediated disease, and as controls in assays for the identification of competitive CCR1 antagonists.
    Type: Grant
    Filed: May 9, 2011
    Date of Patent: July 9, 2013
    Assignee: ChemoCentryx, Inc.
    Inventors: Lianfa Li, Andrew M. K. Pennell, Penglie Zhang
  • PDE-10 inhibitors
    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
  • Bicyclic heterocyclyl derivatives as FGFR kinase inhibitors for therapeutic use
    Patent number: 8481531
    Abstract: The invention relates to new bicyclic heterocyclyl derivatives of formula (I), to pharmaceutical compositions comprising said compounds and to the use of said compounds in the treatment of diseases, e.g. cancer.
    Type: Grant
    Filed: April 15, 2010
    Date of Patent: July 9, 2013
    Assignee: Astex Therapeutics Ltd
    Inventors: Gordon Saxty, Valerio Berdini, Eddy Jean Edgard Freyne, Alexandra Papanikos, Pascal Benderitter, Werner Constant Johan Embrechts, Berthold Wroblowski, Rhalid Akkari
  • NOVEL BENZENESULFONAMIDE COMPOUNDS, METHOD FOR SYNTHESIZING SAME, AND USE THEREOF IN MEDICINE AS WELL AS IN COSMETICS
    Publication number: 20130172363
    Abstract: Benzenesulfonamide compounds having a structure of formula (I) are described. Also described, are methods for synthesizing the compounds and to the use thereof in pharmaceutical compositions for human or veterinary medicine and in cosmetic compositions.
    Type: Application
    Filed: February 22, 2013
    Publication date: July 4, 2013
    Applicant: GALDERMA RESEARCH & DEVELOPMENT
    Inventor: Galderma Research & Development
  • QUINUCLIDINE ESTERS OF 1-AZAHETEROCYCLYLACETIC ACID AS ANTIMUSCARINIC AGENTS, PROCESS FOR THEIR PREPARATION AND MEDICINAL COMPOSITIONS THEREOF
    Publication number: 20130172302
    Abstract: Compounds of formula (I): wherein A, R1, R2, X, m, and n are as defined in the specification, are selective M3 receptor antagonists and may be used in the treatment of, inter alia, a respiratory disease such as asthma and COPD.
    Type: Application
    Filed: December 28, 2012
    Publication date: July 4, 2013
    Applicant: Chiesi Farmaceutici S.p.A.
    Inventor: Chiesi Farmaceutici S.p.A.
  • DERIVATIVES OF AZAINDAZOLE OR DIAZAINDAZOLE TYPE AS MEDICAMENT
    Publication number: 20130172360
    Abstract: The present invention relates to a compound of following formula (I): or a pharmaceutically acceptable salt or solvate of same, a tautomer of same, or a stereoisomer or mixture of stereoisomers of same in any proportions, such as a mixture of enantiomers, notably a racemic mixture; as well as to the use of same as a drug, notably intended for the treatment of cancer, inflammation and neurodegenerative diseases such as Alzheimer's disease; to the use of same as a kinase inhibitor; to the pharmaceutical compositions comprising same; and to methods for the preparation of same.
    Type: Application
    Filed: January 27, 2012
    Publication date: July 4, 2013
    Applicant: PIERRE FABRE MEDICAMENT
    Inventors: El Bachir Kaloun, Karim Bedjeguelal, Rémi Rabot, Anna Kruczynski, Philippe Schmitt, Michel Perez, Nicolas Rahier
  • IMIDAZOPYRIDINE, IMIDAZOPYRIMIDINE AND IMIDAZOPYRAZINE DERIVATIVES AS MELANOCORTIN-4 RECEPTOR MODULATORS
    Publication number: 20130165426
    Abstract: Disclosed is a compound of Formula I or a salt thereof, in which X, X1, X2, R1, R2, and R3 are described herein. Also disclosed are pharmaceutical compositions and methods of using the compounds of Formula I to treat disorders mediated by melanocortin-4 receptors.
    Type: Application
    Filed: July 5, 2011
    Publication date: June 27, 2013
    Applicant: UNIVERSITÉ DE MONTRÉAL
    Inventors: Réjean Ruel, Yves Chantigny, Anne Marinier, Patricia Rene, Michel Bouvier
  • CHEMICAL COMPOUNDS
    Publication number: 20130165439
    Abstract: The present invention encompasses compounds of general formula (I) wherein the groups R1 to R5 are defined as in claim 1, which are suitable for treating diseases characterised by excessive or abnormal cell proliferation, and their use for preparing a medicament having the above-mentioned properties.
    Type: Application
    Filed: February 25, 2013
    Publication date: June 27, 2013
    Applicant: Boehringer Ingelheim International GmbH
    Inventors: Darryl MCCONNELL, Lars van der VEEN, Tobias WUNBERG
  • Inhibitors of VEGF receptor and HGF receptor signalling
    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
  • Compounds and methods for treatment of cancer
    Patent number: 8470817
    Abstract: Compounds for treating, preventing or managing cancer are disclosed. Also provided are methods for using the compounds in treatment of various cancers. Also provided are methods of treatment using the compounds together with another chemotherapy, radiation therapy, hormonal therapy, biological therapy, or immunotherapy. Pharmaceutical compositions suitable for use in the methods are also disclosed.
    Type: Grant
    Filed: October 26, 2010
    Date of Patent: June 25, 2013
    Assignee: Sunesis Pharmaceuticals, Inc.
    Inventor: Anantha Sudhakar
  • Anellated pyridine compounds
    Patent number: 8470828
    Abstract: The present invention is concerned with novel dual modulators of the 5-HT2A and D3 receptors of formula (I) wherein X, Y, A, R1, R2, and R3 are as described herein, as well as pharmaceutically acceptable salts and esters thereof. Further the present invention is concerned with the manufacture of the compounds of formula (I), pharmaceutical compositions comprising them and their use as therapeutics.
    Type: Grant
    Filed: June 29, 2011
    Date of Patent: June 25, 2013
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Luca Gobbi, Rosa Maria Rodriguez Sarmiento, Juergen Wichmann
  • Compounds and methods for kinase modulation, and indications therefor
    Patent number: 8470818
    Abstract: Compounds active on protein kinases are described, as well as methods of using such compounds to treat diseases and conditions associated with aberrant activity of protein kinases.
    Type: Grant
    Filed: October 18, 2010
    Date of Patent: June 25, 2013
    Assignee: Plexxikon Inc.
    Inventors: Prabha N. Ibrahim, Dean R. Artis, Ryan Bremer, Shumeye Mamo, Chao Zhang, Jiazhong Zhang, Jianming Tsai, Klaus-Peter Hirth, Gideon Bollag, Wayne Spevak, Hanna Cho, Samuel J. Gillette, Shenghua Shi
  • NOVEL COMPOUNDS
    Publication number: 20130158042
    Abstract: This invention relates to compounds of formula I their use as positive allosteric modulators of mGlu5 receptor activity, pharmaceutical compositions containing the same, and methods of using the same as agents for treatment and/or prevention of neurological and psychiatric disorders associated with glutamate dysfunction such as schizophrenia or cognitive decline such as dementia or cognitive impairment. R1, R2, R3, R4, Q have meanings given in the description.
    Type: Application
    Filed: December 10, 2012
    Publication date: June 20, 2013
    Inventors: Annekatrin HEIMANN, Georg DAHMANN, Marc GRUNDL, Stephan Georg MUELLER, Bernd WELLENZOHN
  • Substituted Triazolopyridines
    Publication number: 20130156756
    Abstract: The present invention relates to substituted triazolopyridine compounds of general formula (I): in which R1, R2, R3, R4, and R5 are as given in the description and in the claims, to methods of preparing said compounds, to pharmaceutical compositions and combinations comprising said compounds, to the use of said compounds for manufacturing a pharmaceutical composition for the treatment or prophylaxis of a disease of uncontrolled cell growth, proliferation and/or survival as well as to the use of intermediate compounds for the preparation of said compounds.
    Type: Application
    Filed: June 14, 2011
    Publication date: June 20, 2013
    Applicant: BAYER INTELLECTUAL PROPERTY GMBH
    Inventors: Volker Schulze, Dirk Kosemund, Hartmut Schirok, Benjamin Bader, Philip Lienau, Antje Margret Wengner, Hans Briem, Simon Holton, Gerhard Siemeister, Stefan Prechtl, Marcus Koppitz, Detlef Stöckigt, Olaf Prien
  • PYRAZOLO PYRIDINE DERIVATIVES AS NADPH OXIDASE INHIBITORS
    Publication number: 20130158027
    Abstract: The present invention is related to pyrazolo pyridine derivatives of Formula (I), pharmaceutical composition thereof and to their use for the treatment and/or prophylaxis of disorders or conditions related to Nicotinamide adenine dinucleotide phosphate oxidase (NADPH Oxidase).
    Type: Application
    Filed: January 31, 2013
    Publication date: June 20, 2013
    Applicant: GENKYOTEX SA
    Inventor: GENKYOTEX SA
  • AZOLOPYRIDIN-3-ONE DERIVATIVES AS INHIBITORS OF LIPASES AND PHOSPHOLIPASES
    Publication number: 20130157941
    Abstract: The present invention relates to azolopyridin-3-one derivatives of the general formula (I) with the meanings specified in the description, to their pharmaceutically usable salts and to their use as drug substances.
    Type: Application
    Filed: June 17, 2011
    Publication date: June 20, 2013
    Applicant: Sanofi
    Inventors: Stefan Petry, Norbert Tennagels, Karl-Heinz Baringhaus
  • 6-(4-Hydroxy-phenyl)-1H-pyrazolo[3,4-b]pyridine-4-carboxylic acid amide derivatives as kinase inhibitors
    Publication number: 20130150340
    Abstract: The present invention relates to 1H-pyrazolo[3,4-b]pyridine compounds of the formula I, in which R1, R2, R3 and R4 are defined as indicated below. The compounds of the formula I are kinase inhibitors, and are useful for the treatment of diseases associated with diabetes and diabetic complications, such as, diabetic nephropathy, diabetic neuropathy and diabetic retinopathy, 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: October 25, 2012
    Publication date: June 13, 2013
    Applicant: SANOFI
    Inventor: SANOFI
  • KINASE INHIBITORS
    Publication number: 20130150343
    Abstract: Compounds of formula (I) and pharmaceutically acceptable salts thereof: wherein R2, W, A, Y and R1 are as defined in the specification, are p38 MAPK inhibitors, and are useful as anti-inflammatory agents in the treatment of, inter alia, diseases of the respiratory tract.
    Type: Application
    Filed: December 7, 2012
    Publication date: June 13, 2013
    Applicant: Chiesi Farmaceutici S.p.A.
    Inventor: Chiesi Farmaceutici S.p.A.
  • KINASE INHIBITORS
    Publication number: 20130150361
    Abstract: Compounds of formula (I): wherein R2, W, A, Y, and R1 are as defined in the specification, and pharmaceutically acceptable salts thereof, are p38 MAPK inhibitors, and are useful as anti-inflammatory agents in the treatment of, inter alia, diseases of the respiratory tract.
    Type: Application
    Filed: December 7, 2012
    Publication date: June 13, 2013
    Applicant: Chiesi Farmaceutici S.p.A.
    Inventor: Chiesi Farmaceutici S.p.A.
  • ORAL CONTROLLED RELEASE PHARMACEUTICAL COMPOSITIONS OF BLONANSERIN
    Publication number: 20130143897
    Abstract: An oral controlled release pharmaceutical composition comprising Blonanserin and release controlling agent(s) and optionally pharmaceutically acceptable excipients is provided. The present invention further relates to a controlled release pharmaceutical composition comprising Blonanserin and release controlling agent(s) such that the composition releases not less than about 80% of Blonanserin within 20 hours, when dissolution is carried out in 900 ml, 0.1 N HCl, USP apparatus Type II (Paddle) at 50 rpm for 20 hrs. The controlled release pharmaceutical composition of the invention releases 50% of Blonanserin between about 4 to 14 hours, when dissolution is carried out in 900 ml, 0.1 N HCl, USP apparatus Type II (Paddle) at 50 rpm.
    Type: Application
    Filed: August 10, 2011
    Publication date: June 6, 2013
    Applicant: LUPIN LIMITED
    Inventors: Pravin Meghrajji Bhutada, Ashish Ashokrao Deshmukh, Sajeev Chandran, Shirishkumar Kulkarni
  • PYRAZOLO PYRIDINE DERIVATIVES AS NADPH OXIDASE INHIBITORS
    Publication number: 20130143879
    Abstract: The present invention is related to pyrazolo pyridine derivatives of Formula (I), pharmaceutical composition thereof and to their use for the treatment and/or prophylaxis of disorders or conditions related to Nicotinamide adenine dinucleotide phosphate oxidase (NADPH Oxidase).
    Type: Application
    Filed: January 31, 2013
    Publication date: June 6, 2013
    Applicant: GENKYOTEX SA
    Inventor: Genkyotex Sa
  • Selected inhibitors of protein tyrosine kinase activity
    Patent number: 8455484
    Abstract: The invention provides new compounds and compositions thereof. The invention also provides methods for treating ophthalmic diseases, disorders and conditions.
    Type: Grant
    Filed: April 8, 2011
    Date of Patent: June 4, 2013
    Assignee: MethylGene Inc.
    Inventors: Stéphane Raeppel, Lijie Zhan, Stephen William Claridge, Franck Raeppel, Frédéric Gaudette, Arkadii Vaisburg
  • Novel Functionally Selective Ligands of Dopamine D2 Receptors
    Publication number: 20130137679
    Abstract: The present invention relates to novel functionally selective ligands of dopamine D2 receptors, FIG. 1 including agonists, antagonists, and inverse agonists. The invention further relates to the use of these compounds for treating central nervous system disorders related to D2 receptors.
    Type: Application
    Filed: July 1, 2011
    Publication date: May 30, 2013
    Inventors: Jian Jin, Bryan Roth, Stephen Frye
  • Thienopyridine Derivatives for the Treatment and Prevention of Dengue Virus Infections
    Publication number: 20130129677
    Abstract: Methods and pharmaceutical compositions for treating viral infections, by administering certain thienopyridine derivative compounds in therapeutically effective amounts are disclosed. Methods of using the compounds and pharmaceutical compositions thereof are also disclosed. In particular, the treatment of viral infections such as caused by flavivirus is disclosed, i.e., including but not limited to, Dengue virus, West Nile virus, yellow fever virus, Japanese encephalitis virus, and tick-borne encephalitis virus.
    Type: Application
    Filed: December 7, 2012
    Publication date: May 23, 2013
    Applicant: Siga Technologies, Inc.
    Inventor: Siga Technologies, Inc.
  • HETEROCYCLIC COMPOUNDS, THEIR PREPARATION AND THERAPEUTIC APPLICATION
    Publication number: 20130123271
    Abstract: The invention is directed to certain novel compounds, methods for producing them and methods for treating or ameliorating a kinase-mediated disorder.
    Type: Application
    Filed: June 22, 2011
    Publication date: May 16, 2013
    Applicant: FOVEA PHARMACEUTICALS
    Inventors: David Middlemiss, Caroline Leriche
  • Pyrazolo Pyridine Derivatives as NADPH Oxidase Inhibitors
    Publication number: 20130123256
    Abstract: The present invention is related to pyrazolo pyridine derivatives of Formula (I), pharmaceutical composition thereof and to their use for the treatment and/or prophylaxis of disorders or conditions related to Nicotinamide adenine dinucleotide phosphate oxidase (NADPH Oxidase).
    Type: Application
    Filed: January 4, 2013
    Publication date: May 16, 2013
    Applicant: GENKYOTEX SA
    Inventor: Genkyotex Sa
  • NOVEL CYCLIC AZABENZIMIDAZOLE DERIVATIVES USEFUL AS ANTI-DIABETIC AGENTS
    Publication number: 20130123237
    Abstract: Novel compounds of structural formula (I) are activators of AMP-protein kinase and are useful in the treatment, prevention and suppression of diseases mediated by the AMPK-activated protein kinase. The compounds of the present invention are useful in the treatment of Type 2 diabetes, hyperglycemia, metabolic syndrome, obesity, hypercholesterolemia, and hypertension.
    Type: Application
    Filed: February 23, 2012
    Publication date: May 16, 2013
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Rajan Anand, James M. Apgar, Tesfaye Biftu, Ping Chen, Lin Chu, Vincent J. Colandrea, Guizhen Dong, James F. Dropinski, Danqing Feng, Jacqueline D. Hicks, Jinlong Jiang, Alexander J. Kim, Kenneth J. Leavitt, Bing Li, Xiaoxia Qian, Iyassu Sebhat, Lan Wei, Robert R. Wilkening, Zhicai Wu
  • Imidazopyridin-2-one derivatives
    Patent number: 8436012
    Abstract: A compound represented by formula (I) having mTOR inhibitory activity or a pharmacologically acceptable salt thereof.
    Type: Grant
    Filed: November 24, 2010
    Date of Patent: May 7, 2013
    Assignee: Daiichi Sankyo Company, Limited
    Inventors: Masami Ohtsuka, Noriyasu Haginoya, Masanori Ichikawa, Hironori Matsunaga, Hironao Saito, Yoshihiro Shibata, Tomoyuki Tsunemi
  • Pyrrolopyridine inhibitors of kinases
    Patent number: 8435980
    Abstract: The present invention relates to compounds of formula (I) or pharmaceutical acceptable salts, wherein R1a, R1b, R1c, X, and Y are defined in the description. The present invention relates also to compositions containing said compounds which are useful for inhibiting kinases such as Cdc7 and methods of treating diseases such as cancer.
    Type: Grant
    Filed: July 15, 2010
    Date of Patent: May 7, 2013
    Assignee: AbbVie Inc.
    Inventors: Alan S. Florjancic, Yunsong Tong, Thomas D. Penning, Jane Gong, Magdalena Przytulinska, Douglas Steinman, James Holms, Chunqiu Lai, Gui-Dong Zhu, Keith Woods
  • Compounds that interact with glucokinase regulatory protein for the treatment of diabetes
    Patent number: 8431563
    Abstract: The present invention relates to compounds of Formula I, or pharmaceutically acceptable salts thereof, that interact with glucokinase regulatory protein. In addition, the present invention relates to methods of treating type 2 diabetes, and other diseases and/or conditions where glucokinase regulatory protein is involved using the compounds, or pharmaceutically acceptable salts thereof, and pharmaceutical compositions that contain the compounds, or pharmaceutically acceptable salts thereof.
    Type: Grant
    Filed: August 23, 2011
    Date of Patent: April 30, 2013
    Assignee: Amgen Inc.
    Inventors: Kate Ashton, Michael David Bartberger, Yunxin Bo, Marian C. Bryan, Michael Croghan, Christopher Harold Fotsch, Clarence Henderson Hale, Roxanne Kay Kunz, Longbin Liu, Nobuko Nishimura, Mark H. Norman, Lewis Dale Pennington, Steve Fong Poon, Markian Myroslaw Stec, David Joseph St. Jean, Jr., Nuria A. Tamayo, Christopher Michael Tegley, Kevin Chao Yang
  • COMPOUNDS AND METHODS FOR TREATING INFLAMMATORY AND FIBROTIC DISORDERS
    Publication number: 20130102597
    Abstract: Disclosed are compounds and methods for treating inflammatory and fibrotic disorders, including methods of modulating a stress activated protein kinase (SAPK) system with an active compound, wherein the active compound exhibits low potency for inhibition of the p38 MAPK; and wherein the contacting is conducted at a SAPK-modulating concentration that is at a low percentage inhibitory concentration for inhibition of the p38 MAPK by the compound. Also disclosed are derivatives and analogs of pirfenidone, useful for modulating a stress activated protein kinase (SAPK) system.
    Type: Application
    Filed: October 15, 2012
    Publication date: April 25, 2013
    Applicant: INTERMUNE, INC.
    Inventor: INTERMUNE, INC.
  • OXAZOLE TYROSINE KINASE INHIBITORS
    Publication number: 20130102592
    Abstract: The invention provides a compound which is an amide of the formula (1), or a salt, solvate, N-oxide or tautomer thereof; wherein: a is 0 or 1; b is 0 or 1: provided that the sum of a and b is 0 or 1; T is O or NH Ar1 is a monocyclic or bicyclic 5- to 10-membered aryl or heteroaryl group containing up to 4 heteroatoms selected from O, N and S, and being optionally substituted en by one or more substituents R1; Ar2 Js a monocyclic or bicyclic 5- to 10-membered aryl or heteroaryl group containing up to 4 heteroatoms selected from O, N and S and being optionally substituted by one or more substituents R2; and R1 and R2 are as defined in the claims. The compounds are inhibitors of kinases and in particular FLT3, FLT4 and Aurora kinases.
    Type: Application
    Filed: December 5, 2012
    Publication date: April 25, 2013
    Applicant: SAREUM LIMITED
    Inventor: Sareum Limited
  • THIOAMIDE, AMIDOXIME AND AMIDRAZONE DERIVATIVES AS HIV ATTACHMENT INHIBITORS
    Publication number: 20130102615
    Abstract: A compound of Formula I, including pharmaceutically acceptable salts thereof: wherein A is selected from the group of:
    Type: Application
    Filed: April 11, 2012
    Publication date: April 25, 2013
    Inventors: Nicholas A. Meanwell, Tao Wang, Zhongxing Zhang, Lawrence G. Hamann, John F. Kadow
  • New Enzyme Inhibitor Compounds
    Publication number: 20130102587
    Abstract: Disclosed are compounds which inhibit SSAO enzyme activity. Also disclosed are pharmaceutical compositions comprising these compounds and the use of these compounds in the treatment or prevention of medical conditions wherein inhibition of SSAO activity is beneficial, such as inflammatory diseases, immune disorders and the inhibition of tumour growth.
    Type: Application
    Filed: March 14, 2011
    Publication date: April 25, 2013
    Applicant: PROXIMAGEN LIMITED
    Inventors: David Evans, Allison Carley, Alison Stewart, Michael Higginbottom, Edward Savory, Iain Simpson, Marianne Nilsson, Martin Haraldsson, Erik Nordling, Tobias Koolmeister
  • Inhibitors of Protein Tyrosine Kinase Activity
    Publication number: 20130096088
    Abstract: The present invention provides new compounds and methods for treating a disease responsive to inhibition of kinase activity, for example a disease responsive to inhibition of protein tyrosine kinase activity, for example a disease responsive to inhibition of protein tyrosine kinase activity of growth factor receptors, for example a disease responsive to inhibition of receptor type tyrosine kinase signaling, or for example, a disease responsive to inhibition of VEGF receptor signaling.
    Type: Application
    Filed: September 27, 2012
    Publication date: April 18, 2013
    Applicant: METHYLGENE INC.
    Inventor: METHYLGENE INC.
  • Heterocyclic Compounds for the Treatment of Neurological and Psychological Disorders
    Publication number: 20130096089
    Abstract: Lactam compounds of Formula I and their use for the treatment of neurological and psychiatric disorders including schizophrenia, bipolar disorder, anxiety disorder and insomnia is disclosed.
    Type: Application
    Filed: September 7, 2012
    Publication date: April 18, 2013
    Inventors: Julius F. Remenar, Laura Cook Blumberg, Tarek A. Zeidan
  • Inhibitors of Protein Tyrosine Kinase Activity
    Publication number: 20130096136
    Abstract: The present invention provides new compounds and methods for treating a disease responsive to inhibition of kinase activity, for example a disease responsive to inhibition of protein tyrosine kinase activity, for example a disease responsive to inhibition of protein tyrosine kinase activity of growth factor receptors, for example a disease responsive to inhibition of receptor type tyrosine kinase signaling, or for example, a disease responsive to inhibition of VEGF receptor signaling.
    Type: Application
    Filed: September 27, 2012
    Publication date: April 18, 2013
    Applicant: METHYLGENE INC.
    Inventor: METHYLGENE INC.
  • OPTICAL CORRECTION
    Publication number: 20130096131
    Abstract: The present disclosure describes compositions which improve visual acuity and to methods for their use.
    Type: Application
    Filed: December 3, 2012
    Publication date: April 18, 2013
    Inventor: Anant SHARMA
  • Selected Inhibitors of Protein Tyrosine Kinase Activity
    Publication number: 20130096135
    Abstract: The present invention provides new compounds and methods for treating a disease responsive to inhibition of kinase activity, for example a disease responsive to inhibition of protein tyrosine kinase activity, for example a disease responsive to inhibition of protein tyrosine kinase activity of growth factor receptors, for example a disease responsive to inhibition of receptor type tyrosine kinase signaling, or for example, a disease responsive to inhibition of VEGF receptor signaling.
    Type: Application
    Filed: September 27, 2012
    Publication date: April 18, 2013
    Applicant: METHYLGENE INC.
    Inventor: MethylGene Inc.
  • Pyrrolidinyl-alkyl-amide derivatives, their preparation, and their therapeutic application as CCR3 receptor ligands
    Patent number: 8420636
    Abstract: The present invention relates to pyrrolidinyl-alkyl-amide derivatives of formula (I) or (IA) wherein the variables are as defined herein, to their preparation and to their therapeutic use as CCR3 receptor ligands.
    Type: Grant
    Filed: January 26, 2011
    Date of Patent: April 16, 2013
    Assignee: Sanofi
    Inventors: Agnes Behr, Sandor Batori, Veronika Bartane Bodor, Zoltan Szlavik, Imre Bata, Katalin Urban-Szabo, Zoltan Kapui, Endre Mikus
  • Inhibitors of Protein Tyrosine Kinase Activity
    Publication number: 20130090327
    Abstract: The present invention provides new compounds and methods for treating a disease responsive to inhibition of kinase activity, for example a disease responsive to inhibition of protein tyrosine kinase activity, for example a disease responsive to inhibition of protein tyrosine kinase activity of growth factor receptors, for example a disease responsive to inhibition of receptor type tyrosine kinase signaling, or for example, a disease responsive to inhibition of VEGF receptor signaling.
    Type: Application
    Filed: September 27, 2012
    Publication date: April 11, 2013
    Applicant: METHYLGENE INC.
    Inventor: METHYLGENE INC.
  • Cyclic (aza)indolizinecarboxamides, their preparation and their use as pharmaceuticals
    Patent number: 8415336
    Abstract: The present invention relates to cyclic indolizinecarboxamides and azaindolizinecarboxamides of the formulae Ia and Ib, wherein R, Ra, R10, R20, R30, R40, Y, n, p and q have the meanings indicated in the claims, which are valuable pharmaceutical active compounds. Specifically, they inhibit the enzyme renin and modulate the activity of the renin-angiotensin system, and are useful for the treatment of diseases such as hypertension, for example. The invention furthermore relates to processes for the preparation of the compounds of the formulae Ia and Ib, their use and pharmaceutical compositions comprising them.
    Type: Grant
    Filed: January 19, 2012
    Date of Patent: April 9, 2013
    Assignee: Sanofi
    Inventors: Henning Steinhagen, Bodo Scheiper, Hans Matter, Gary McCort, Guillaume Begis, Pascale Goberville, Berangere Thiers
  • 6-(4-Hydroxy-phenyl)-3-alkyl-1H-pyrazolo[3,4-b]pyridine-4-carboxylic acid amide derivatives as kinase inhibitors
    Publication number: 20130085128
    Abstract: The present invention relates to pyrazolo[3,4-b]pyridine compounds of the formula I, in which R1, R2, R3, R4, R5, R6 and R7 are defined as indicated below. The compounds of the formula I are kinase inhibitors, and are useful for the treatment of diseases associated with diabetes and diabetic complications, such as, diabetic nephropathy, diabetic neuropathy and diabetic retinopathy, 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 27, 2012
    Publication date: April 4, 2013
    Applicant: SANOFI
    Inventor: SANOFI
  • DERIVATIVES OF AZAINDAZOLE OR DIAZAINDAZOLE TYPE AS MEDICAMENT
    Publication number: 20130085144
    Abstract: The present invention relates to a compound of following formula (I): or a pharmaceutically acceptable salt or solvate of same, a tautomer of same, or a stereoisomer or mixture of stereoisomers of same in any proportions, such as a mixture of enantiomers, notably a racemic mixture; as well as to the use of same as a drug, notably intended for the treatment of cancer, inflammation and neurodegenerative diseases such as Alzheimer's disease; to the use of same as a kinase inhibitor; to the pharmaceutical compositions comprising same; and to methods for the preparation of same.
    Type: Application
    Filed: November 27, 2012
    Publication date: April 4, 2013
    Applicant: PIERRE FABRE MEDICAMENT
    Inventor: PIERRE FABRE MEDICAMENT
  • ANTI-INFLAMMATORY COMPOUND HAVING INHIBITORY ACTIVITY AGAINST MULTIPLE TYROSINE KINASES AND PHARMACEUTICAL COMPOSITION CONTAINING SAME
    Publication number: 20130072482
    Abstract: The present invention is for the anti-inflammatory compounds that have an inhibitory activity against protein tyrosine kinases and their pharmaceutical composition(s) containing the compound as the active ingredient. Since the compounds of the present invention can inhibit multiple protein kinases associated with inflammatory diseases and immune disorders, they are useful for their prevention or treatment.
    Type: Application
    Filed: May 26, 2011
    Publication date: March 21, 2013
    Inventors: Beom-Seok Yang, Yong-Zu Kim, Tae-Kyo Park, Sung-Ho Woo, Hyang-Sook Lee, Sun-Young Kim, Jong-Un Cho, Hong-Bum Lee