The Additional Six-membered Hetero Ring Is One Of The Cyclos In A Bicyclo Ring System Patents (Class 544/362)
Quinoline or isoquinoline (including hydrogenated) (Class 544/363)
  • 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
  • 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.
  • 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.
  • 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
  • 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.
  • DEUTERATED HIV ATTACHMENT INHIBITORS
    Publication number: 20130096305
    Abstract: Deuterated piperazine and piperidine HIV attachment inhibitor compounds are set forth. The present invention provides compounds of Formula I, the pharmaceutically acceptable salts and/or solvates (e.g., hydrates) thereof, their pharmaceutical formulations, and their use in patients suffering from or susceptible to a virus such as HIV. The compounds of Formula I, their pharmaceutically acceptable salts and/or solvates are effective antiviral agents, particularly as inhibitors of HIV. They are useful for the treatment of HIV and AIDS.
    Type: Application
    Filed: June 15, 2011
    Publication date: April 18, 2013
    Inventors: Tao Wang, Nicholas A. Meanwell, Zhongxing Zhang
  • 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
  • Benzenesulfonamide compounds, method for synthesizing same, and use thereof in medicine as well as in cosmetics
    Patent number: 8420632
    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: Grant
    Filed: June 28, 2010
    Date of Patent: April 16, 2013
    Assignee: Galderma Research & Developlment
    Inventors: Laurence Clary, Sandrine Chambon, Laurent Chantalat, Carine Rosignoli, Olivier Roye, Jean-Claude Pascal, Marléne Schuppli
  • 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.
  • Bronchodilating diazaheteroaryls
    Patent number: 8415333
    Abstract: The invention relates to novel compounds having the general formula (I), and which compounds are useful to treat a disorder or disease characterized by bronchoconstriction, e.g. COPD and asthma.
    Type: Grant
    Filed: February 24, 2010
    Date of Patent: April 9, 2013
    Assignee: Respiratorious AB
    Inventors: Martin Johansson, Viveca Thornqvist Otlner, Jorgen Toftered, David Wensbo, Maria Dalence
  • 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
  • Compounds and methods for kinase modulation, and indications therefor
    Patent number: 8415469
    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: November 10, 2009
    Date of Patent: April 9, 2013
    Assignee: Plexxikon Inc.
    Inventors: Prabha N. Ibrahim, Dean R. Artis, Ryan Bremer, Gaston Habets, Shumeye Mamo, Marika Nespi, Chao Zhang, Jiazhong Zhang, Yong-Liang Zhu, Rebecca Zuckerman, Brian West, Yoshisa Suzuki, Jianming Tsai, Klaus-Peter Hirth, Gideon Bollag, Wayne Spevak, Hanna Cho, Samuel J. Gillette, Guoxian Wu, Hongyao Zhu, Shenghua Shi
  • 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
  • 6-(4-HYDROXY-PHENYL)-3-STYRYL-1H-PYRAZOLO[3,4-b]PYRIDINE-4-CARBOXYLIC ACID AMIDE DERIVATIVES AS KINASE INHIBITORS
    Publication number: 20130065894
    Abstract: The present invention relates to pyrazolo[3,4-b]pyridine compounds of the formula I, in which R1, R2, R3, R4 and R5 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 12, 2011
    Publication date: March 14, 2013
    Applicant: SANOFI
    Inventors: Matthias LOEHN, Maria MENDEZ-PEREZ, Stefania PFEIFFER-MAREK, Aimo KANNT, Guillaume BEGIS, Olivier DUCLOS, Federic JEANNOT
  • Anti-Infective Compounds
    Publication number: 20130065884
    Abstract: The present invention relates to small molecule compounds and their use in the treatment of bacterial infections, in particular Tuberculosis.
    Type: Application
    Filed: March 18, 2011
    Publication date: March 14, 2013
    Inventors: Zaesung No, Jaeseung Kim, Priscille Brodin, Min Jung Seo, Young Mi Kim, Jonathan Cechetto, Heekyoung Jeon, Auguste Genovesio, Saeyeon Lee, Sunhee Kang, Fanny Anne Ewann, Ji Youn Nam, Thierry Christophe, Denis Philippe Cedric Fenistein, Heo Jamung, Jang Jiyeon
  • Triazolo [4, 5- B] Pyridin Derivatives
    Publication number: 20130065883
    Abstract: There is provided compounds of formula (I), wherein R1, R2, R3 and R4 have meanings given in the description, and pharmaceutically-acceptable esters, amides, solvates or salts thereof, which compounds are useful in the treatment of diseases in which inhibition of a protein or lipid kinase (e.g. a PIM family kinase, such as PIM-1, PIM-2 and/or PIM-3, and/or Flt3) is desired and/or required, and particularly in the treatment of cancer or a proliferative disease.
    Type: Application
    Filed: February 18, 2011
    Publication date: March 14, 2013
    Applicant: Centro Nacional de Investigaceiones Oncologicas (CNIO)
    Inventors: Joaquin Pastor Fernández, Julen Oyarzabal Santamarina, Carl-Gustaf Pierre Saluste, Carmen Blanco Aparicio, Rosa Maria Alvarez Escobar, Virginia Rivero Buceta
  • Benzophenone hybrids as anticancer agents and processes for the preparation thereof
    Patent number: 8394954
    Abstract: Disclosed herein are benzophenone hybrids with potent anticancer activities and processes for creation of the same.
    Type: Grant
    Filed: March 26, 2008
    Date of Patent: March 12, 2013
    Assignee: Council of Scientific & Industrial Research
    Inventors: Ahmed Kamal, Bandari Rajendra Prasad
  • BICYCLIC AGONISTS OF GPR131 AND USES THEREOF
    Publication number: 20130059845
    Abstract: The present disclosure relates to compounds that act as agonists of, or otherwise modulate the activity of, GPR131 and to their use in the treatment of various diseases. In particular embodiments, the structure of the compounds is given by Formula I: wherein the variables are as described herein. Related compositions, formulations and methods for the preparation of compounds of formula I are also described.
    Type: Application
    Filed: August 24, 2012
    Publication date: March 7, 2013
    Inventors: Jiangao SONG, Phuongly Pham, Jingyuan Ma, Aaron Robert Novack, Imad Nashashibi, David W. G. Wone, Dong-Fang Shi, Xin Chen
  • COMPOUNDS AND COMPOSITIONS AS C-KIT KINASE INHIBITORS
    Publication number: 20130059846
    Abstract: The invention provides compounds and pharmaceutical compositions thereof, which are useful as protein kinase inhibitors, as well as methods for using such compounds to treat, ameliorate or prevent a condition associated with abnormal or deregulated kinase activity. In some embodiments, the invention provides methods for using such compounds to treat, ameliorate or prevent diseases or disorders that involve abnormal activation of c-kit or c-kit and PDGFR (PDGFR?, PDGFR?) kinases.
    Type: Application
    Filed: August 27, 2012
    Publication date: March 7, 2013
    Applicant: IRM LLC
    Inventors: Vince YEH, Xiaolin LI, Xiaodong LIU, Jon LOREN, Valentina MOLTENI, Juliet NABAKKA, Bao NGUYEN, Hank Michael James PETRASSI
  • COMPOUNDS AND COMPOSITIONS AS C-KIT KINASE INHIBITORS
    Publication number: 20130059832
    Abstract: The invention provides compounds and pharmaceutical compositions thereof, which are useful as protein kinase inhibitors, as well as methods for using such compounds to treat, ameliorate or prevent a condition associated with abnormal or deregulated kinase activity. In some embodiments, the invention provides methods for using such compounds to treat, ameliorate or prevent diseases or disorders that involve abnormal activation of c-kit or c-kit and PDGFR (PDGFR?, PDGFR?) kinases.
    Type: Application
    Filed: August 29, 2012
    Publication date: March 7, 2013
    Inventors: Valentina MOLTENI, Hank Michael James PETRASSI, Xiaolin LI, Xiaodong LIU, Jon LOREN, Juliet NABAKKA, Bao NGUYEN, Vince YEH
  • AZAINDAZOLES
    Publication number: 20130059849
    Abstract: Herein are disclosed azaindazoles of formula (I) where the various groups are defined herein, and which are useful for treating cancer.
    Type: Application
    Filed: May 5, 2011
    Publication date: March 7, 2013
    Inventors: Joelle Lorraine Burgess, Neil Johnson, Steven D. Knight, Louis Lafrance, William H. Miller, Kenneth Newlander, Stuart Romeril, Meagan B. Rouse, Xinrong Tian, Sharad Kumar Verma, Dominic Suarez
  • Pyrazolo pyridine derivatives as NADPH oxidase inhibitors
    Patent number: 8389518
    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: Grant
    Filed: March 20, 2008
    Date of Patent: March 5, 2013
    Assignee: Genkyotex SA
    Inventors: Patrick Page, Mike Orchard, Laetitia Fioraso-Cartier, Bianca Mottironi
  • PYRAZOLOPYRIDINE KINASE INHIBITORS
    Publication number: 20130053395
    Abstract: The present invention relates to compounds useful as inhibitors of protein kinase. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders. The invention also provides processes for preparing compounds of the inventions.
    Type: Application
    Filed: July 27, 2012
    Publication date: February 28, 2013
    Applicant: VERTEX PHARMACEUTICALS INCORPORATED
    Inventors: Juan-Miguel Jimenez, Julian M.C. Golec, Luca Settimo, Damien Fraysse, Guy Brenchley, Dean Boyall, Heather Twin, Stephen Young, Andrew W. Miller, Christopher John Davis, Philip N. Collier
  • 5-HT RECEPTOR MODULATORS
    Publication number: 20130053372
    Abstract: The invention relates to compounds of formula (I), useful for treating disorders mediated by the 5-hydroxytryptamine (serotonin) receptor IB (5-HT1B), e.g. vascular disorders, cancer and CNS disorders. The invention also provides methods of treating such disorders, and compounds and compositions etc. for their treatment.
    Type: Application
    Filed: February 15, 2011
    Publication date: February 28, 2013
    Inventors: Prashant Bhimrao Kapadnis, Robert Glen, Robin Hiley, James Bell, David Spring
  • Azaindazole compounds and methods of use
    Patent number: 8383630
    Abstract: Provided are methods for the treatment of rheumatoid arthritis using compounds of formula Ia and Ib: or a pharmaceutically acceptable salt, hydrate or N-oxide thereof.
    Type: Grant
    Filed: July 1, 2010
    Date of Patent: February 26, 2013
    Assignee: Chemocentryx, Inc.
    Inventors: Penglie Zhang, Andrew M. K. Pennell, John J. Kim Wright, Wei Chen, Manmohan R. Leleti, Yandong Li, Lianfa Li, Yuan Xu
  • 1,6-disubstituted-3-amino-4,5,6,7-tetrahydro-1H-pyrazolo[3,4-C]pyridin-7-one compounds and preparation thereof
    Patent number: 8383631
    Abstract: Provided are a novel 1,6-disubstituted-4,5,6,7-tetrahydro-1H-pyrazolo[3,4-c]pyridin-7-one compound, a pharmaceutically acceptable salt compound thereof, a method for preparing the compound, and an anticancer pharmaceutical composition including the compound as an effective ingredient.
    Type: Grant
    Filed: September 16, 2010
    Date of Patent: February 26, 2013
    Assignee: Korea Institute of Science and Technology
    Inventors: Ghilsoo Nam, Ae Nim Pae, Kyung Il Choi, Hyunah Choo, Vani Nelamane Devegowda, Seon Hee Seo
  • TYPE II RAF KINASE INHIBITORS
    Publication number: 20130040949
    Abstract: The present invention relates to novel compounds which are able to modulate b-raf kinases, and the use of such compounds in the treatment of various diseases, disorders or conditions.
    Type: Application
    Filed: December 29, 2010
    Publication date: February 14, 2013
    Applicant: DANA-FARBER CANCER INSTITUTE, INC.
    Inventors: Nathanael S. Gray, Hwan G. Choi, Xianming Deng, Jianming Zhang
  • PYRAZOLO[3,4-c]PYRIDINE COMPOUNDS AND METHODS OF USE
    Publication number: 20130039906
    Abstract: Pyrazolo[3,4-c]pyridine compounds of Formula I, including stereoisomers, geometric isomers, tautomers, and pharmaceutically acceptable salts thereof, wherein R1 and R2 are as defined herein, are useful for inhibiting Pim kinase, and for treating disorders such as cancer mediated by Pim kinase. Methods of using compounds of Formula I for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed.
    Type: Application
    Filed: August 10, 2012
    Publication date: February 14, 2013
    Inventors: Steven Do, Huiyong Hu, Aleksandr Kolesnikov, Wendy Lee, Vickie H. Tsui, Xiaojing Wang, Zhaoyang Wen
  • NOVEL AMIDE DERIVATIVE AND USE THEREOF AS MEDICINE
    Publication number: 20130040930
    Abstract: Provided are a novel low-molecular-weight compound that suppresses production of induction type MMPs, particularly MMP-9, rather than production of hemostatic type MMP-2, as well as a prophylactic/therapeutic drug for autoimmune diseases or osteoarthritis. An amide derivative represented by the following formula (I) wherein each symbol is as defined in the specification, or a pharmacologically acceptable salt thereof.
    Type: Application
    Filed: April 27, 2011
    Publication date: February 14, 2013
    Applicant: MITSUBISHI TANABE PHARMA CORPORATION
    Inventors: Kazuhiro Maeda, Jun-ichi Endoh, Akiko Tarao, Kaoru Tashiro, Seigo Ishibuchi, Hidemasa Hikawa
  • 8-ethyl-6-(aryl)pyrido[2,3-D]pyrimidin-7(8H)-ones for the treatment of CNS disorders
    Patent number: 8372970
    Abstract: Provided herein are PAK inhibitors and methods of utilizing PAK inhibitors for the treatment of CNS disorders such as neuropsychiatric disorders.
    Type: Grant
    Filed: October 8, 2010
    Date of Patent: February 12, 2013
    Assignee: Afraxis, Inc.
    Inventors: Benedikt Vollrath, David Campbell, Sergio G. Durón, Warren Wade
  • Pyrazolopyridines as kinase inhibitors
    Patent number: 8372842
    Abstract: Compounds of Formula I are useful for inhibition of CHK1 and/or CHK2. Methods of using compounds of Formula I and stereoisomers and pharmaceutically acceptable salts thereof, for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions are disclosed.
    Type: Grant
    Filed: January 8, 2009
    Date of Patent: February 12, 2013
    Assignee: Array BioPharma Inc.
    Inventors: James F. Blake, Indrani W. Gunawardana, Yvan Le Huerou, Peter J. Mohr, Eli M. Wallace, Bin Wang
  • HETEROCYCLIC COMPOUNDS AND USES THEREOF
    Publication number: 20130035324
    Abstract: Heterocyclic entities that modulate PI3 kinase activity, pharmaceutical compositions containing the heterocyclic entities, and methods of using these chemical entities for treating diseases and conditions associated with PI3 kinase activity are described herein.
    Type: Application
    Filed: August 17, 2010
    Publication date: February 7, 2013
    Inventors: Pingda Ren, Yi Liu, Liansheng Li, Katrina Chan, Troy Edward Wilson, Simon Fraser Campbell
  • Substituted 1,3-Benzothiazol-2(3H)-Ones and [1,3]Thiazolo[5,4-B]Pyridin-2(IH)-Ones as Positive Allosteric Modulators of MGLUR2
    Publication number: 20130035332
    Abstract: The present invention is directed to benzothiazol-one and thiazolo pyridine-one 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 25, 2011
    Publication date: February 7, 2013
    Inventors: Mark E. Layton, Michael J. Kelly
  • THERAPEUTICALLY ACTIVE COMPOSITIONS AND THEIR METHODS OF USE
    Publication number: 20130035329
    Abstract: Compounds and compositions comprising compounds useful in the treatment of cancer are described herein.
    Type: Application
    Filed: June 8, 2012
    Publication date: February 7, 2013
    Inventors: Jeffrey O. Saunders, Francesco G. Salituro
  • Organic compounds
    Patent number: 8367662
    Abstract: Compounds of formula I: in free or salt or solvate form, where R1, R2, R3 and R20 have the meanings as indicated in the specification, are useful for treating diseases mediated by the ALK-5 and/or ALK-4 receptor. Pharmaceutical compositions that contain the compounds and processes for preparing the compounds are also described. These compounds are useful for the treatment of inflammatory or obstructive airways diseases such as pulmonary hypertension, pulmonary fibrosis, liver fibrosis, cancer, muscle diseases such as muscle atrophies and muscle dystrophies, and systemic skeletal disorders such as osteoporosis.
    Type: Grant
    Filed: October 15, 2008
    Date of Patent: February 5, 2013
    Assignee: Novartis AG
    Inventors: Duncan Shaw, Catherine Leblanc, Dimitrios Lizos, Cathy Ritchie, Vikki Furminger, Sarah Lewis, Benoit Hornsperger, Nikolaus Johannes Stiefl, Sven Weiler
  • Azetidinyl diamides as monoacylglycerol lipase inhibitors
    Patent number: 8367653
    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 Y, Z, R1, and s are defined herein.
    Type: Grant
    Filed: April 22, 2010
    Date of Patent: February 5, 2013
    Assignee: Janssen Pharmaceutica NV
    Inventors: Haiyan Bian, Kristen Chevalier, Jose Clemente, Pete Connolly, Chris Flores, Shu-Chen Lin, Li Liu, John Mabus, Mark MacIelag, Mark McDonnell, Philip Pitis, Yue-Mei Zhang, Sui-Po Zhang, Bin Zhu
  • 3-carbamoyl-2-pyridone derivatives
    Patent number: 8367666
    Abstract: The present invention provides compounds having an agonistic activity to the cannabinoid receptor, which is represented by the formula (I): wherein R1, R2, R3, R4, and G are defined as herein, a pharmaceutically acceptable salt or a solvate thereof, and pharmaceutical compositions, atopic dermatitis treating agents, and anti-pruritus agents, especially anti-pruritus agents for oral used and for external application, which each contains the said compound as an active ingredient.
    Type: Grant
    Filed: February 28, 2012
    Date of Patent: February 5, 2013
    Assignee: Shionogi & Co., Ltd.
    Inventors: Takashi Sasatani, Yoshiharu Hiramatsu, Susumu Mitsumori
  • AZAINDOLYLPHENYL SULFONAMIDES AS SERINE/THREONINE KINASE INHIBITORS
    Publication number: 20130029993
    Abstract: The present invention encompasses compounds of general formula (I) wherein the groups R2 to R6, A, X, Y and m are defined as in claim 1, which are suitable for the treatment of diseases characterised by excessive or abnormal cell proliferation, pharmaceutical preparations which contain compounds of this kind and their use as medicaments.
    Type: Application
    Filed: January 27, 2012
    Publication date: January 31, 2013
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventor: Heinz Stadtmueller
  • METHODS OF MAKING HIV ATTACHMENT INHIBITOR PRODRUG COMPOUND AND INTERMEDIATES
    Publication number: 20130030178
    Abstract: A method for making the compound of Formula I: is set forth using alkylation, amidation, chlorination and phosphate installation procedures.
    Type: Application
    Filed: January 27, 2012
    Publication date: January 31, 2013
    Inventors: Jonathan Clive Tripp, Dayne Dustan Fanfair, Mitchell J. Schultz, Saravanababu Murugesan, Richard J. Fox, Chung-Pin H. Chen, Sabrina E. Ivy, Joseph Francis Payack, Wendel W. Doubleday
  • CXCR3 receptor antagonists
    Patent number: 8362249
    Abstract: The present invention relates to compounds of formula (I): and pharmaceutically acceptable salts thereof, wherein R1 to R6, A, B, X, Y and n are as defined herein. The invention also relates to pharmaceutical compositions comprising these compounds, methods of using these compounds in the treatment of various diseases and disorders, processes for preparing these compounds and intermediates useful in these processes.
    Type: Grant
    Filed: April 21, 2010
    Date of Patent: January 29, 2013
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: John David Ginn, Daniel Richard Marshall, Anthony S. Prokopowicz, Sabine Schlyer, Robert Sibley, Michael Robert Turner, Di Wu, Frank Wu
  • Azetidinyl diamides as monoacylglycerol lipase inhibitors
    Patent number: 8362000
    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 Y, Z, R1, and s are defined herein.
    Type: Grant
    Filed: April 22, 2010
    Date of Patent: January 29, 2013
    Assignee: Janssen Pharmaceutica NV
    Inventors: Haiyan Bian, Kristen Chevalier, Jose Clemente, Pete Connolly, Chris Flores, Shu-Chen Lin, Li Liu, John Mabus, Mark Macielag, Mark McDonnell, Philip Pitis, Yue-Mei Zhang, Sui-Po Zhang, Bin Zhu
  • Thyazolopyridin-2-yloxy-phenyl and thiazolopyrazin-2-yloxy-phenyl amines as modulators of leukotriene A4 hydrolase
    Patent number: 8357684
    Abstract: Thiazolopyridin-2-yloxy-phenyl and thiazolopyrazin-2-yloxy-phenyl amine compounds are described, which are useful as LTA4 hydrolase (LTA4H) modulators. Such compounds may be used in pharmaceutical compositions and methods for modulation of LTA4H and for the treatment of disease states, disorders, and conditions mediated by LTA4 hydrolase activity.
    Type: Grant
    Filed: March 2, 2011
    Date of Patent: January 22, 2013
    Assignee: Janssen Pharmaceutica NV
    Inventors: Genesis M. Bacani, Eugene Y. Cheung, Christa C. Chrovian, Laurent Gomez, Cheryl A. Grice, Aaron M. Kearney, Adrienne M. Landry-Bayle, Alice Lee-Dutra, Alejandro Santillán, Jr., Kathleen Sappey, Kia Sepassi, Virginia M. Tanis, Alvah T. Wickboldt, John J. M. Wiener
  • Acetylenic Heteroaryl Compounds
    Publication number: 20130018046
    Abstract: This invention relates to compounds of the general formula: in which the variable groups are as defined herein, and to their preparation and use.
    Type: Application
    Filed: September 13, 2012
    Publication date: January 17, 2013
    Applicant: ARIAD Pharmaceuticals, Inc.
    Inventors: Yihan Wang, Xiaotian Zhu, Rajeswari Sundaramoorthi, Wei-Sheng Huang, Dong Zou, R. Mathew Thomas, Jiwei Qi, Jan Antoinette C. Romero, David C. Dalgarno, William C. Shakespeare, Tomi K. Sawyer, Chester A. Metcalf, III
  • NOVEL ANXIOLYTIC COMPOUNDS
    Publication number: 20130012508
    Abstract: The present invention relates to chemical compounds of general formula (I) which may possess useful therapeutic activity in a range of central nervous system disorders, and in particular, anxiety disorders.
    Type: Application
    Filed: September 14, 2012
    Publication date: January 10, 2013
    Applicant: Bionomics Limited
    Inventors: Jonathan Bayldon Baell, Brad Sleebs, Bernard Luke Flynn, Ian Phillip Street, Nurul Quazi, Chinh Thien Bui
  • Substituted Imidazopyridinyl-Aminopyridine Compounds
    Publication number: 20120329791
    Abstract: The present invention relates to substituted imidazopyridinyl-aminopyridine compounds and methods of synthesizing these compounds. The present invention also relates to pharmaceutical compositions containing substituted imidazopyridinyl-aminopyridine compounds and methods of treating cell proliferative disorders, such as cancer, by administering these compounds and pharmaceutical compositions to subjects in need thereof.
    Type: Application
    Filed: June 21, 2012
    Publication date: December 27, 2012
    Applicant: ArQuele, Inc.
    Inventors: Mark A. Ashwell, Chris Brassard, Anton Filikov, Jason Hill, Steffi Koerner, Jean-Marc Lapierre, Yanbin Liu, Nivedita Namdev, Robert Nicewonger, Rocio Palma, Manish Tandon, David Vensel, Akihisa Matsuda, Shin Iimura, Kenichi Yoshida, Takanori Yamazaki, Takahiro Kitamura, Takeshi Isoyama
  • TRIAZOLOPYRIDINES
    Publication number: 20120328610
    Abstract: The present invention relates to triazolopyridine compounds of general formula (I) which are Monopolar Spindle 1 kinase (Mps-1 or TTK) inhibitors: 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 proliferative of diseases, as well as to intermediate compounds useful in the preparation of said compounds.
    Type: Application
    Filed: November 17, 2010
    Publication date: December 27, 2012
    Applicant: BAYER INTELLECTUAL PROPERTY GMBH
    Inventors: Volker Schulze, Marcus Koppitz, Dirk Kosemund, Hartmut Schirok, Benjamin Bader, Philip Lienau, Antje Margret Wengner, Hans Briem, Simon Holton, Gerhard Siemeister, Stefan Prechtl, Ulf Bömer
  • NOVEL BENZENESULFONAMIDE COMPOUNDS, METHOD FOR SYNTHESIZING SAME, AND USE THEREOF IN MEDICINE AS WELL AS IN COSMETICS
    Publication number: 20120323006
    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: June 28, 2010
    Publication date: December 20, 2012
    Applicant: GALDERMA RESEARCH & DEVELOPMENT
    Inventors: Laurence Clary, Sandrine Chambon, Laurent Chantalat, Carine Rosignoli, Olivier Roye, Jean-Claude Pascal, Marlene Schuppli
  • Compounds, pharmaceutical compositions and uses thereof
    Publication number: 20120322784
    Abstract: The present invention relates to compounds of formula I, wherein the groups R1, LP, LQ, X1, X2, X3, Ar and n are as defined in the application, which have valuable pharmacological properties, and in particular bind to the GPR119 receptor and modulate its activity.
    Type: Application
    Filed: December 16, 2011
    Publication date: December 20, 2012
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: Frank HIMMELSBACH, Matthias ECKHARDT, Niklas HEINE, Elke LANGKOPF, Bernd NOSSE