Carbocyclic Ring Bonded Directly To The Nitrogen Patents (Class 544/165)
  • Patent number: 9409922
    Abstract: The disclosure generally relates to compounds of formula I, including compositions and methods for treating human immunodeficiency virus (HIV) infection. The disclosure provides novel inhibitors of HIV, pharmaceutical compositions containing such compounds, and methods for using these compounds in the treatment of HIV infection.
    Type: Grant
    Filed: February 11, 2015
    Date of Patent: August 9, 2016
    Assignee: Bristol-Myers Squibb Company
    Inventors: Kevin Peese, Zhongyu Wang, John F. Kadow, Prasanna Sivaprakasam, B. Narasimhulu Naidu
  • Patent number: 9284288
    Abstract: The present invention relates to 1-(p-tolyl)cyclopropyl substituted bridged spiro[2.4]heptane derivatives of formula (I), wherein R1 is as defined in the description, their preparation and their use as pharmaceutically active compounds.
    Type: Grant
    Filed: May 15, 2013
    Date of Patent: March 15, 2016
    Assignee: ACTELION PHARMACEUTICALS LTD.
    Inventors: Olivier Corminboeuf, Sylvaine Cren
  • Publication number: 20150080400
    Abstract: The compounds of formula (1) in which R1, R4, A and X have the meanings as given in the description, are novel effective EP2 agonists.
    Type: Application
    Filed: April 30, 2013
    Publication date: March 19, 2015
    Applicant: TAKEDA GMBH
    Inventors: Angelika Hoffmeyer, Rainer Boer, Manuela Hessmann, Andreas Pahl, Torsten Dunkern, Simone Hartung, Christof Zitt, Jurgen Volz, Christiane Praechter, Mahindra Makhija, Hiteshkumar Jain, Sandip Gavade, Arati Prabhu, Manojkumar Tiwari, Ashish Keche, Sarvesh Patel
  • Publication number: 20150072980
    Abstract: The present invention is directed to compounds, their synthesis, and their use as antagonists, inverse agonists, modulators and or inhibitors of the Retinoic acid-related orphan nuclear receptor ?t (ROR?t)/ROR?. The compounds of the present invention are useful for modulating ROR?t)/ROR? activity and for treating diseases or conditions mediated by ROR?t)/ROR? such as for example, disease states associated with immunopathology of human autoimmune diseases such as Multiple Sclerosis (MS), Rheumatoid Arthritis (RA), Inflammatory Colitis, Psoriasis, COPD, Pain, Obesity, Diabetes, Dyslipidemia, Osteoporosis, Asthma, Neurodegenerative diseases and Cancer.
    Type: Application
    Filed: August 27, 2014
    Publication date: March 12, 2015
    Inventors: Hariprasad Vankayalapati, Venkatakrishnareddy Yerramreddy
  • Publication number: 20140352081
    Abstract: The present invention relates to a para-aminophenol compound of formula (I) the addition salts thereof with an acid and the solvates thereof, dye composition comprising the latter and a dyeing process.
    Type: Application
    Filed: September 13, 2012
    Publication date: December 4, 2014
    Applicant: L'OREAL
    Inventor: Aziz Fadli
  • Publication number: 20140357628
    Abstract: Substituted cinnamoyl anthranilate compounds exhibiting anti-fibrotic activity; or derivatives thereof, analogues thereof, pharmaceutically acceptable salts thereof, and metabolites thereof, with the proviso that the compound is no Tranilast.
    Type: Application
    Filed: June 27, 2014
    Publication date: December 4, 2014
    Applicant: Fibrotech Therapeutics Pty Ltd
    Inventors: Spencer John Williams, David Stapleton, Steven Zammit, Darren James Kelly, Richard Ernest Gilbert, Henry Krum
  • Publication number: 20140350019
    Abstract: The present invention relates to aniline derivatives of formula (I), to their preparation and to their therapeutic application, for example in treating glaucoma: Formula (I), R1a represents H, an halogen, a (C1-C6)alkyl or a CN; R1b represents H, an halogen or a (C1-C6)alkyl; R1c represents H or a (C1-C6)alkyl; R2 represents H, an halogen, an OH, an O—(C1-C6)alkyl or (C1-C6)alkyl; R3 represents H, an halogen, a (C1-C6)alkyl, an OH, an O—(C1-C6)alkyl, a CONH2 or CN; R4 represents H, an halogen or a (C1-C6)alkyl; R5 represents H or F: R7 represents H or F; R8 represents H or F; R9 represents H or (C1-C6)alkyl, or one of its enantiomers.
    Type: Application
    Filed: September 7, 2012
    Publication date: November 27, 2014
    Applicant: FOVEA PHARMACEUTICALS
    Inventors: John Feutrill, Caroline Leriche, David Middlemiss
  • Patent number: 8889678
    Abstract: The present invention relates to acyl guanidine derivatives modulating the hedgehog protein signaling pathway to be used as drugs, in particular for treating diseases involving a tissue dysfunction associated with a deregulation of the hedgehog protein signaling pathway, as well as to pharmaceutical compositions containing same. The present invention also relates to novel acyl guanidine derivatives as such.
    Type: Grant
    Filed: July 19, 2010
    Date of Patent: November 18, 2014
    Assignees: Centre National de la Recherche Scientifique, Universite de Strasbourg
    Inventors: Martial Ruat, Hélène Faure, Elisabeth Traiffort, Hermine Roudaut, André Mann, Angèle Schoenfelder, Maurizio Taddei, Fabrizio Manetti, Antonio Solinas
  • Publication number: 20140336185
    Abstract: Compounds that bind the glucagon-like peptide 1 (GLP-1) receptor, methods of their synthesis, methods of their therapeutic and/or prophylactic use, and methods of their use in stabilizing GLP-1 receptor in vitro for crystallization of the GLP-1 receptor are provided. Certain compounds may have activity as modulators or potentiators with respect to glucagon receptor, GIP receptor, GLP-1 and GLP-2 receptors, and PTH receptor on their own or in the presence of receptor ligands such as GIP (1-42), PTH (1-34), Glucagon (1-29), GLP-2 (1-33), GLP-1 (7-36), GLP-1 (9-36), oxyntomodulin and exendin variants.
    Type: Application
    Filed: May 31, 2012
    Publication date: November 13, 2014
    Inventors: Marcus F. Boehm, Esther Martinborough, Manisha Moorjani, Junko Tamiya, Liming Huang, Thomas Fowler, Andrew Novak, Premji Meghani, Enugurthi Brahmachary, Adam Richard Yeager
  • Patent number: 8871976
    Abstract: The invention includes a compound represented by the following structural formula: wherein is described herein. The compounds of the invention are useful in staining embryonic stem cells.
    Type: Grant
    Filed: August 26, 2011
    Date of Patent: October 28, 2014
    Assignees: National University of Singapore, Agency for Science, Technology and Research
    Inventors: Young-Tae Chang, Sung Chan Lee, Nam Young Kang
  • Patent number: 8853281
    Abstract: Compounds of the formula I wherein R1a is H; and R1b is C1-C6 alkyl, Carbocyclyl or Het; or R1a and R1b together define a saturated cyclic amine with 3-6 ring atoms; R2a and R2b are H, halo, C1-C4alkyl, C1-C4haloalkyl, C1-C4alkoxy; or R2a and R2b together with the carbon atom to which they are attached form a C3-C6cycloalkyl; R3 is a branched C5-C10alkyl chain, C2-C4haloalkyl or C3-C7cycloalkylmethyl, R4 is Het, Carbocyclyl, optionally substituted as defined in the specification and pharmaceutically acceptable salts, hydrates and N-oxides thereof; are inhibitors of cathepsin S and have utility in the treatment of psoriasis, autoimmune disorders and other disorders such as asthma, arteriosclerosis, COPD and chronic pain.
    Type: Grant
    Filed: December 18, 2009
    Date of Patent: October 7, 2014
    Assignee: Medivir UK Ltd
    Inventors: Susana Ayesa, Anna Karin Belfrage, Bjorn Classon, Urszula Grabowska, Ellen Hewitt, Vladimir Ivanov, Daniel Jönsson, Pia Kahnberg, Peter Lind, Magnus Nilsson, Lourdes Odén, Mikael Pelcman, Horst Wähling
  • Publication number: 20140296343
    Abstract: Methods and compounds for treating neurological and other disorders are provided. Included is the administering to a subject in need thereof an effective amount of a compound having binding and/or modulation specificity for a TrkB receptor molecule.
    Type: Application
    Filed: March 31, 2014
    Publication date: October 2, 2014
    Inventors: Frank M. LONGO, Stephen M. MASSA, Sandeep GUPTA
  • Publication number: 20140296241
    Abstract: The disclosure provides pharmaceutical preparations containing (2R,6R)-hydroxynorketamine, or (R)- or (S)-dehydronorketamine, or other stereoisomeric dehydro or hydroxylated ketamine metabolite. (2R,6R)-hydroxynorketamine The disclosure also provides novel ketamine metabolite prodrugs. The disclosure provides methods of treating, bipolar depression, major depressive disorder, neuropathic and chronic pain, including complex regional pain disorder (CRPS) by administering a purified ketamine metabolite or a ketamine metabolite prodrug directly to patients in need of such treatment.
    Type: Application
    Filed: October 15, 2012
    Publication date: October 2, 2014
    Inventors: Irving W. Wainer, Ruin Moaddel, Michel Bernier, Carlos A. Zarate, Marc C. Torjman, Michael E. Goldberg, Mary J. Tanga
  • Publication number: 20140219989
    Abstract: The present invention provides a compound of Formula (I) as described herein, or a pharmaceutically acceptable salt thereof. The present invention also provides pharmaceutical compositions comprising one or more said compounds, and methods for using said compounds for treating or preventing a thromboses, embolisms, hypercoagulability or fibrotic changes.
    Type: Application
    Filed: July 3, 2012
    Publication date: August 7, 2014
    Inventors: Craig Boyle, William Greenlee, Samuel Chackalamannil, Claire Lankin
  • Publication number: 20140200197
    Abstract: The compounds encompassed by Formula I include compounds which are HIV protease inhibitors and other compounds which can be metabolized in vivo to HIV protease inhibitors. The compounds and their pharmaceutically acceptable salts are useful for the prophylaxis or treatment of infection by HIV and the prophylaxis, treatment, or delay in the onset of AIDS. The compounds and their salts can be employed as ingredients in pharmaceutical compositions, optionally in combination with other antivirals, immunomodulators, antibiotics or vaccines.
    Type: Application
    Filed: September 9, 2013
    Publication date: July 17, 2014
    Inventors: JOHN A. MCCAULEY, CHRISTIAN BEAULIEU, DAVID J. BENNETT, CHRISTOPHER J. BUNGARD, RONALD K. CHANG, SHELDON CRANE, THOMAS J. GRESHOCK, LI HAO, KATE HOLLOWAY, JESSE J. MANIKOWSKI, DANIEL MCKAY, CARMELA MOLINARO, OSCAR MIGUEL MORADEI, PHILIPPE G. NANTERMET, CHRISTIAN NADEAU, TUMMANAPALLI SATYANARAYANA, WILLIAM SHIPE, SANJAY KUMAR SINGH, VOUY LINH TRUONG, SIVALENKA VIJAYARADHI, PETER D. WILLIAMS, CATHERINE M. WISCOUNT
  • Patent number: 8772478
    Abstract: Benzenesulfonamide compounds having a structure of the following general 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: July 8, 2014
    Assignee: Galderma Research & Development
    Inventors: Laurence Clary, Sandrine Chambon, Laurent Chantalat, Pascale Mauvais, Olivier Roye, Marlène Schuppli
  • Patent number: 8765812
    Abstract: Substituted cinnamoyl anthranilate compounds exhibiting anti-fibrotic activity; or derivatives thereof, analogues thereof, pharmaceutically acceptable salts thereof, and metabolites thereof; with the proviso that the compound is not Tranilast.
    Type: Grant
    Filed: July 5, 2007
    Date of Patent: July 1, 2014
    Assignee: Fibrotech Therapeutics Pty Ltd
    Inventors: Spencer John Willams, David Stapleton, Steven Zammit, Darren James Kelly, Richard Ernest Gilbert, Henry Krum
  • Publication number: 20140179660
    Abstract: An N1-cyclic amine-N5-substituted phenyl biguanide derivative of Formula 1 or a pharmaceutically acceptable salt thereof, a method of manufacturing the same, and a pharmaceutical composition including the biguanide derivative or the pharmaceutically acceptable salt thereof as an active ingredient are provided. The biguanide derivatives have an effect of inhibiting cancer cell proliferation and also exhibit anticancer activity including inhibition of cancer metastasis and cancer recurrence, because they are effective in activating AMPK, which is associated with the control of energy metabolism, even when administered in a small dose compared with conventional drugs. Also, the biguanide derivatives are highly effective at lowering blood glucose and lipid concentration by AMPK activation, thus they may be effectively used to treat diabetes mellitus, obesity, hyperlipemia, hypercholesterolemia, fatty liver, coronary artery disease, osteoporosis, polycystic ovary syndrome and metabolic syndrome.
    Type: Application
    Filed: August 8, 2012
    Publication date: June 26, 2014
    Applicant: HANALL BIOPHARMA CO., LTD.
    Inventors: Sung Wuk Kim, Chang Hee Min, Se Hwan Park, Duck Kim, Ji Sun Lee, Yong Eun Kim, Ju Hoon Oh
  • Publication number: 20140171404
    Abstract: The present invention relates to novel compounds that are autotaxin inhibitors, processes for their preparation, pharmaceutical compositions and medicaments containing them and to their use in the treatment of an ATX-dependent or ATX-mediated disease or condition.
    Type: Application
    Filed: December 17, 2013
    Publication date: June 19, 2014
    Applicant: NOVARTIS AG
    Inventors: Vikki FURMINGER, Owen Rhys HUGHES, Darren Mark LEGRAND, Emily STANLEY, Christopher THOMSON
  • Publication number: 20140081017
    Abstract: The present invention relates to compositions and methods to selectively treat fungal infection. More particularly, the invention relates to compounds, compositions thereof, and methods for selectively enhancing fungal sensitivity to antifungal compounds.
    Type: Application
    Filed: March 14, 2013
    Publication date: March 20, 2014
    Applicant: METHYLGENE INC.
    Inventor: METHYLGENE INC.
  • Patent number: 8673903
    Abstract: The present application relates to novel substituted 8-alkoxy-2-aminotetraline derivatives, to processes for their preparation, to their use for the treatment and/or prevention of diseases and to their use for preparing medicaments for the treatment and/or prevention of diseases, in particular for the treatment and/or prevention of cardiovascular disorders.
    Type: Grant
    Filed: May 9, 2011
    Date of Patent: March 18, 2014
    Assignee: Bayer Intellectual Property GmbH
    Inventors: Walter Hübsch, Michael Hahn, Alexandros Vakalopoulos, Volkhart Min-Jian Li, Frank Wunder, Johannes-Peter Stasch, Karl-Heinz Schlemmer, Friederike Stoll, Niels Lindner
  • Patent number: 8648071
    Abstract: The present invention relates to substituted hydrazonamide compounds. The invention further relates to methods of inhibiting the activity of Hs?90 in a subject in need thereof and methods for treating hyperproliferative disorders, such as cancer, in a subject in need thereof comprising administering to the subject a substituted hydrazonamide compound of the invention, or a pharmaceutical composition comprising such a compound.
    Type: Grant
    Filed: June 26, 2009
    Date of Patent: February 11, 2014
    Assignee: Synta Pharmaceuticals Corp.
    Inventors: Joseph Burlison, Dinesh U. Chimmanamada, Weiwen Ying, Shijie Zhang, David James
  • Patent number: 8642576
    Abstract: Compounds of formula Ia and Ib wherein A, B, C and R1 are described herein.
    Type: Grant
    Filed: August 29, 2012
    Date of Patent: February 4, 2014
    Assignee: Bristol-Myers Squibb Company
    Inventors: Mark E. Salvati, Heather Finlay, Bang-Chi Chen, Lalgudi S. Harikrishnan, Ji Jiang, James A. Johnson, Muthoni G. Kamau, R. Michael Lawrence, Jianqing Li, John Lloyd, Michael M. Miller, Zulan Pi, Jennifer X. Qiao, Richard A. Rampulla, Jacques Y. Roberge, Tammy C. Wang, Yufeng Wang, Wu Yang
  • Publication number: 20140011807
    Abstract: The present invention provides a nitrogen-containing saturated heterocyclic compound of the formula [I]: wherein R1 is a cycloalkyl group and the like, R22 is an optionally substituted aryl and the like, R is a lower alkyl and the like, T is a carbonyl group, Z is —O— and the like, and R3 to R6 are the same or different and a hydrogen atom and the like; or a pharmaceutically acceptable salt, that is useful as a renin inhibitor.
    Type: Application
    Filed: March 15, 2012
    Publication date: January 9, 2014
    Applicants: SHANGHAI PHARMACEUTICALS HOLDING CO., LTD., MITSUBISHI TANABE PHARMA CORPORATION
    Inventors: Toru Iijima, Hiroshi Sugama, Takayuki Kawaguchi, Jingkang Shen, Guangxin Xia, Jianshu Xie
  • Publication number: 20130331392
    Abstract: The invention provides cycloalkyl guanidine compounds that inhibit F1F0-ATPase, and methods of using cyclalkyl guanidine compounds as therapeutic agents in therapy, such as treating an immune disorder, inflammatory condition, or cancer.
    Type: Application
    Filed: December 8, 2011
    Publication date: December 12, 2013
    Inventors: Alexander R. Hurd, Clarke B. Taylor, Peter L. Toogood, Chad A. Van Huis
  • Patent number: 8563714
    Abstract: The present invention relates to bridged spiro[2.4]heptane derivatives of formula (I), wherein W, Y, Z, R1 and R2 are as defined in the description, their preparation and their use as pharmaceutically active compounds as ALX receptor and/or FPRL2 agonists for the treatment of inflammatory and obstructive airways diseases.
    Type: Grant
    Filed: May 17, 2010
    Date of Patent: October 22, 2013
    Assignee: Actelion Pharmaceuticals Ltd.
    Inventors: Daniel Bur, Olivier Corminboeuf, Sylvaine Cren, Corinna Grisostomi, Xavier Leroy, Sylvia Richard-Bildstein
  • Publication number: 20130224790
    Abstract: The invention includes a compound represented by the following structural formula: wherein is described herein. The compounds of the invention are useful in staining embryonic stem cells.
    Type: Application
    Filed: August 26, 2011
    Publication date: August 29, 2013
    Applicants: AGENCY FOR SCIENCE, TECHNOLOGY AND RESEARCH, NATIONAL UNIVERSITY OF SINGAPORE
    Inventors: Young-Tae Chang, Sung Chan Lee, Nam Young Kang
  • Patent number: 8519188
    Abstract: The present invention relates to a compound of general formula (I): and also to the pharmaceutically acceptable salts thereof, to the isomers or isomer mixtures thereof in all proportions, in particular to an enantiomer mixture, and especially to a racemic mixture. The present invention also relates to the use of these compounds as a medicament, and in particular for the treatment of cancer, and also to the compositions containing them.
    Type: Grant
    Filed: June 15, 2009
    Date of Patent: August 27, 2013
    Assignee: Marc-Henry Pitty
    Inventors: Denis Carniato, Karine Jaillardon, Olivier Busnel, Mathieu Gutmann, Jean-Francois Briand, Benoit Deprez, Dominique Thomas, Cécile Bougeret
  • Publication number: 20130217692
    Abstract: Provided is a compound represented by formula (1) or a pharmacologically acceptable salt thereof. (In the formula, A is C6-10 arylene, etc.; R1a, R1b and R1c each independently is a hydrogen atom, a halogen atom, a C1-4 alkyl group, a C1-4 alkoxy group, etc.; R2 is an optionally substituted C6-10 aryl group, an optionally substituted 5- to 12-membered monocyclic or polycyclic heteroaryl group, an optionally substituted C7-16 aralkyl group, etc.; m is 0, etc.; n is an integer of 0 to 2.
    Type: Application
    Filed: September 2, 2011
    Publication date: August 22, 2013
    Applicant: DAINIPPON SUMITOMO PHARMA CO., LTD.
    Inventors: Yoshihiro Horiuchi, Hiroaki Fujiwara, Hitoshi Suda, Izumi Sasaki, Mitsutaka Iwata, Kiyoto Sawamura
  • Publication number: 20130203751
    Abstract: The present application relates to novel substituted 8-alkoxy-2-aminotetraline derivatives, to processes for their preparation, to their use for the treatment and/or prevention of diseases and to their use for preparing medicaments for the treatment and/or prevention of diseases, in particular for the treatment and/or prevention of cardiovascular disorders.
    Type: Application
    Filed: May 9, 2011
    Publication date: August 8, 2013
    Applicant: BAYER INTELLECTUAL PROPERTY GMBH
    Inventors: Walter Hübsch, Michael Hahn, Alexandros Vakalopoulos, Volkhart Min-Jian Li, Frank Wunder, Johannes-Peter Stasch, Karl-Heinz Schlemmer, Friederike Stoll, Niels Lindner
  • Publication number: 20130203738
    Abstract: The present invention identifies a compound which binds to the PAH1 domain of mSin3B that specifically binds to neural restrictive silencer factor NRSF, and uses the compound as a prophylactic and/or a therapeutic for diseases associated with abnormal expression of neural restrictive silencer factor NRSF/REST or abnormal expression of genes targeted by NRSF/REST, such as Huntington's disease, medulloblastoma and neuropathic pain. The present invention provides a pharmaceutical composition comprising a substance capable of binding to the PAH1 domain of mSin3B, e.g.
    Type: Application
    Filed: February 9, 2011
    Publication date: August 8, 2013
    Applicants: NAGOYA CITY UNIVERSITY, NAGASAKI UNIVERSITY
    Inventors: Yoshifumi Nishimura, Aritaka Nagadoi, Yuuka Hirao, Yoshio Goshima, Naoya Yamashita, Naoki Miyata, Takayoshi Suzuki, Ryuta Hiraishi, Hiroshi Ueda
  • Patent number: 8501991
    Abstract: The present invention relates to compounds which activate the p53 response, and find use in, for example, hyperproliferative diseases such as cancer treatment and potentially other diseases/conditions (involving sirtuin function).
    Type: Grant
    Filed: September 4, 2007
    Date of Patent: August 6, 2013
    Assignees: University Court of the University of Dundee, University Court of the University of St. Andrews
    Inventors: Sonia Lain, David Phillip Lane, Michael John Raymond Stark, Anna Rose McCarthy, Jonathan James Hollick, Nicholas James Westwood
  • Publication number: 20130178457
    Abstract: Compounds of Formula (I) along with processes for their preparation that are useful for treating, managing and/or lessening the diseases, disorders, syndromes or conditions associated with the modulation of cannabinoid (CB) receptors. Methods of treating, managing and/or lessening the diseases, disorders, syndromes or conditions associated with the modulation of cannabinoid (CB) receptors of Formula (I).
    Type: Application
    Filed: July 5, 2012
    Publication date: July 11, 2013
    Applicant: LUPIN LIMITED
    Inventors: Sanjeev Anant KULKARNI, Sachin MADAN, Nirmal Kumar JANA, Prashant Vitthalrao TALE, Narasimha Murthy CHEEMALA, Sachin Jaysing MAHANGARE, Prashant Popatrao VIDHATE, Chaitanya Prabhakar KULKARNI, Sapana Suresh PATEL, Amolsing Dattu PATIL, Seema Prabhakar ZADE, Rohan Mahadev SHINDE, Venkata P. PALLE, Rajender Kumar KAMBOJ
  • Patent number: 8470831
    Abstract: Acrylamido derivatives useful as therapeutic agents, particularly for the prevention and/or treatment of diseases and conditions associated with the activity of the mitochondrial permeability transition pore (MPTP), such as the diseases characterized by ischemia/reperfusion, oxidative or degenerative tissue damage, are herein described. These compounds belong to the structural formula (I) wherein R, R?, R?, W and a are as defined in the specification. The invention also relates to the preparation of these compounds, as well as to pharmaceutical compositions comprising them.
    Type: Grant
    Filed: September 23, 2009
    Date of Patent: June 25, 2013
    Assignee: Cogenia SRL
    Inventors: Daniele Fancelli, Mario Varasi, Simon Plyte, Marco Ballarini, Anna Cappa, Giacomo Carenzi, Saverio Minucci, Gilles Pain, Manuela Villa
  • Publication number: 20130137690
    Abstract: The present invention relates to a novel class of 4-carboxybenzylamino derivatives. The 4-carboxybenzylamino compounds can be used to treat cancer. The 4-carboxybenzylamino compounds can also inhibit histone deacetylase and are suitable for use in selectively inducing terminal differentiation, and arresting cell growth and/or apoptosis of neoplastic cells, thereby inhibiting proliferation of such cells. Thus, the compounds of the present invention are useful in treating a patient having a tumor characterized by proliferation of neoplastic cells. The compounds of the invention may also be useful in the prevention and treatment of TRX-mediated diseases, such as autoimmune, allergic and inflammatory diseases, and in the prevention and/or treatment of diseases of the central nervous system (CNS), such as neurodegenerative diseases.
    Type: Application
    Filed: January 28, 2013
    Publication date: May 30, 2013
    Inventors: Paul Harrington, Richard W. Heidebrecht, JR., Solomon Kattar, Thomas A. Miller, Karin M. Otte, Phieng Siliphaivanh, Matthew G. Stanton, Paul Tempest, Kevin J. Wilson, David J. Witter
  • Publication number: 20130029992
    Abstract: The invention provides well defined N,N-dialkylalkenyl ester compounds for treating glaucoma or ocular hypertension. The esters of the invention are particularly advantageous due to their stability in aqueous solutions.
    Type: Application
    Filed: July 25, 2012
    Publication date: January 31, 2013
    Applicant: Allergan, Inc.
    Inventors: Robert M. Burk, David W. Old
  • Publication number: 20120322761
    Abstract: Compounds of formula Ia and Ib wherein A, B, C and R1 are described herein.
    Type: Application
    Filed: August 29, 2012
    Publication date: December 20, 2012
    Inventors: Mark E. Salvati, Heather Finlay, Bang-Chi Chen, Lalgudi S. Harikrishnan, Ji Jiang, James A. Johnson, Muthoni G. Kamau, R. Michael Lawrence, Jianqing Li, John Lloyd, Michael M. Miller, Zulan Pi, Jennifer X. Qiao, Richard A. Rampulla, Jacques Y. Roberge, Tammy C. Wang, Yufeng Wang, Wu Yang
  • Publication number: 20120252801
    Abstract: The present invention relates to a series of novel compounds which have been shown to possess antifungal activity. The invention therefore relates to the new compounds, methods for their preparation, pharmaceutical compositions comprising them and to the compounds for use as a medicament, more in particular antifungal medicament.
    Type: Application
    Filed: December 15, 2010
    Publication date: October 4, 2012
    Applicant: Katholieke Universiteit Leuven, K.U.Leuven R&D
    Inventors: Dorothée Bardiot, Bruno Cammue, Patrick Chaltin, Arnaud Marchand, Karin Thevissen
  • Publication number: 20120196865
    Abstract: The present invention relates to acyl guanidine derivatives modulating the hedgehog protein signaling pathway to be used as drugs, in particular for treating diseases involving a tissue dysfunction associated with a deregulation of the hedgehog protein signaling pathway, as well as to pharmaceutical compositions containing same. The present invention also relates to novel acyl guanidine derivatives as such.
    Type: Application
    Filed: July 19, 2010
    Publication date: August 2, 2012
    Applicants: UNIVERSITE DE STRASBOURG, CENTRE NATIONAL DE LA RECHERCHE SCIENTIFIQUE
    Inventors: Martial Ruat, Hélène Faure, Elisabeth Traiffort, Hermine Roudaut, André Mann, Angèle Schoenfelder, Maurizio Taddei, Fabrizio Manetti, Antonio Solinas
  • Publication number: 20120116072
    Abstract: Benzenesulfonamide compounds having a structure of the following general 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: May 10, 2012
    Inventors: Laurence Clary, Sandrine Chambon, Laurent Chantalat, Pascale Mauvais, Olivier Roye, Marlene Schuppli
  • Publication number: 20120115851
    Abstract: An objective of the present invention is to provide compounds that can effectively suppress the concentration of phosphorus in serum to effectively prevent or treat diseases induced by an increase in concentration of phosphate in serum. The compounds according to the present invention are compounds represented by formula (I) and pharmaceutically acceptable salts and solvates thereof: wherein A represents an optionally substituted five- to nine-membered unsaturated carbocyclic moiety or a five- to nine-membered unsaturated heterocyclic moiety, and represents a single bond or a double bond, R5 represents optionally substituted aryl or the like, Z represents —N?CHR6R7 or the like, R6 and R7 represent H, optionally substituted alkyl, optionally substituted aryl or the like, R101 and R102 together form ?O, and R103 and R104 represent H, or R101 and R104 together from a bond, and R102 and R103 together form a bond.
    Type: Application
    Filed: January 18, 2012
    Publication date: May 10, 2012
    Applicant: KYOWA HAKKO KIRIN CO., LTD.
    Inventors: Nobuaki Eto, Rika Nagao, Tetsuko Kazama
  • Publication number: 20120094971
    Abstract: This invention relates to compounds of Formula (I) wherein Cy1, L1, Y, R1, L2, and Ar2 are defined herein, for the treatment of cancers, inflammatory disorders, and neurological conditions.
    Type: Application
    Filed: September 3, 2009
    Publication date: April 19, 2012
    Applicant: REPLIGEN CORPORATION
    Inventors: James R. Rusche, Norton P. Peet, Allen T. Hopper
  • Publication number: 20120046288
    Abstract: The present invention relates to substituted hydrazonamide compounds. The invention further relates to methods of inhibiting the activity of Hs?90 in a subject in need thereof and methods for treating hyperproliferative disorders, such as cancer, in a subject in need thereof comprising administering to the subject a substituted hydrazonamide compound of the invention, or a pharmaceutical composition comprising such a compound.
    Type: Application
    Filed: June 26, 2009
    Publication date: February 23, 2012
    Inventors: Joseph A. Burlison, Dinesh U. Chimmanamada, Weiwen Ying, Shijie Zhang, David James
  • Publication number: 20120028982
    Abstract: A drug effective for the treatment and prevention of psychiatric disorders such as schizophrenia, anxiety and related ailments thereof, depression, bipolar disorder and epilepsy. The drug antagonizes the action of group II metabotropic glutamate receptors and shows high activity in oral administration. A 2-amino-bicyclo[3.1.0]hexane-2,6-dicarboxylic ester derivative represented by formula [I] [wherein R1 and R2 are identical or different, and each represents a hydrogen atom, a C1-10alkyl group or the like; X represents a hydrogen atom or a fluorine atom; Y represents —OCHR3R4 or the like (wherein R3 and R4 are identical or different, and each represents a hydrogen atom, a C1-10alkyl group or the like; and n represents integer 1 or 2)], a pharmaceutically acceptable salt thereof or a hydrate thereof.
    Type: Application
    Filed: October 7, 2011
    Publication date: February 2, 2012
    Applicant: TAISHO PHARMACEUTICAL CO., LTD.
    Inventors: Akito YASUHARA, Kazunari Sakagami, Hiroshi Ohta, Atsuro Nakazato
  • Publication number: 20120028249
    Abstract: Disclosed are near IR emitting fluorescent compounds; methods of making and kits containing the described compounds; and their use in fluorescence-based detection of biological materials.
    Type: Application
    Filed: October 20, 2009
    Publication date: February 2, 2012
    Applicant: LIFE TECHNOLOGIES CORPORATION
    Inventors: Stephen Yue, Shih-Jung Huang, Jolene Bradford
  • Publication number: 20120004232
    Abstract: A drug effective for the treatment and prevention of psychiatric disorders such as schizophrenia, anxiety and related ailments thereof, depression, bipolar disorder and epilepsy. The drug antagonizes the action of group II metabotropic glutamate receptors and shows high activity in oral administration A 2-amino-bicyclo[3.1.0]hexane-2,6-dicarboxylic ester derivative represented by formula [I] [wherein R1 and R2 are identical or different, and each represents a hydrogen atom, a C1-10alkyl group or the like; X represents a hydrogen atom or a fluorine atom; Y represents —OCHR3R4 or the like (wherein R3 and R4 are identical or different, and each represents a hydrogen atom, a C1-10alkyl group or the like; and n represents integer 1 or 2)], a pharmaceutically acceptable salt thereof or a hydrate thereof.
    Type: Application
    Filed: September 8, 2011
    Publication date: January 5, 2012
    Applicant: TAISHO PHARMACEUTICAL CO., LTD.
    Inventors: Akito YASUHARA, Kazunari SAKAGAMI, Hiroshi OHTA, Atsuro NAKAZATO
  • Publication number: 20120004310
    Abstract: Methods and compounds for treating neurological and other disorders are provided. Included is the administering to a subject in need thereof an effective amount of a compound having binding and/or modulation specificity for a TrkB receptor molecule.
    Type: Application
    Filed: May 27, 2011
    Publication date: January 5, 2012
    Inventors: Frank M. LONGO, Stephen M. Massa, Sandeep Gupta
  • Publication number: 20110312964
    Abstract: Compounds of the formula I wherein R1a is H; and R1b is C1-C6 alkyl, Carbocyclyl or Het; or R1a and R1b together define a saturated cyclic amine with 3-6 ring atoms; R2a and R2b are H, halo, C1-C4alkyl, C1-C4haloalkyl, C1-C4alkoxy; or R2a and R2b together with the carbon atom to which they are attached form a C3-C6cycloalkyl; R3 is a branched C5-C10alkyl chain, C2-C4haloalkyl or C3-C7cycloalkylmethyl, R4 is Het, Carbocyclyl, optionally substituted as defined in the specification and pharmaceutically acceptable salts, hydrates and N-oxides thereof; are inhibitors of cathepsin S and have utility in the treatment of psoriasis, autoimmune disorders and other disorders such as asthma, arteriosclerosis, COPD and chronic pain
    Type: Application
    Filed: December 18, 2009
    Publication date: December 22, 2011
    Applicant: Medivir UK LTD
    Inventors: Susana Ayesa, Anna Karin Belfrage, Björn Classon, Urszula Grabowska, Ellen Hewitt, Vladimir Ivanov, Daniel Jönsson, Pia Kahnberg, Peter Lind, Magnus Nilsson, Lourdes Odén, Mikael Pelcman, Horst Wähling
  • Patent number: 8076332
    Abstract: The present invention relates to a study on the synthesis of a novel N-(2-aminophenyl)benzamide derivative having an urea structure and represented by the general formula (1); and the utilization of a pharmacological effect of the derivative. A compound represented by the general formula (1) or a salt thereof has an effect of cellular morphological change on trabecular meshwork cells and is effective in the prevention and/or treatment of a disease considered to be related to intraocular pressure. In the formula, R1 and R2 represent a hydrogen atom, a lower alkyl group, or the like; R3 represents a hydroxy group, a lower alkoxy group, a lower cycloalkyloxy group, an aryloxy group, or the like; R4 and R5 represent a halogen atom, a lower alkyl group, a hydroxy group, a lower alkoxy group, or the like; X represents a lower alkylene group or the like; Y represents a single bond, a lower alkylene group, or the like; l and m represent 0, 1, 2, or the like.
    Type: Grant
    Filed: December 26, 2007
    Date of Patent: December 13, 2011
    Assignee: Santen Pharmaceutical Co., Ltd.
    Inventors: Hiroyuki Mogi, Hisashi Tajima, Noriko Mishina, Yusuke Yamazaki, Shinji Yoneda, Katsuhiko Watanabe, Junko Fujikawa, Minoru Yamamoto
  • Publication number: 20110275797
    Abstract: An N-acyl anthranilic acid derivative represented by general formula (1) or a salt thereof is useful for prevention or treatment of diseases associated with excessive production of collagen. (In the formula, R1 represents a carboxyl group or the like; R2 represents a hydrogen atom or the like; R3 represents an optionally substituted aryl group or the like; X1 represents a carbonyl group; X2 represents a bonding hand; X3 represents a bonding hand; X4 represents a bonding hand or the like; and A represents an optionally substituted phenyl group or the like.
    Type: Application
    Filed: January 29, 2010
    Publication date: November 10, 2011
    Applicant: Toyama Chemical Co., Ltd.
    Inventors: Junichi Yokotani, Arihiro Takatori, Yukie Tada, Minori Yanai, Hiroshi Kato, Yoichi Taniguchi, Chiharu Tanabe