Isoquinolines (including Hydrogenated) Patents (Class 514/307)
Plural isoquinoline ring systems attached directly or indirectly to each other by nonionic bonding (Class 514/308)
Chalcogen attached directly to the six-membered hetero ring by nonionic bonding (Class 514/309)
Nitrogen, other than as nitro or nitroso, attached directly to the isoquinoline ring system by nonionic bonding (Class 514/310)
  • PROTEASE INHIBITORS
    Publication number: 20120136002
    Abstract: A compound of formula (I) wherein R1 to R15, P1, P2, A, B and Q are as defined in the claims and pharmaceutically acceptable salts and esters thereof, are disclosed. The compounds of formula (I) possess utility as matriptase inhibitors and are useful in the treatment of matriptase dependent conditions, particularly cancer.
    Type: Application
    Filed: May 18, 2010
    Publication date: May 31, 2012
    Inventors: Rajeev Goswami, Anil Kumar Vuppala, Ramesh Veludandi, Ramesh Sistla, Chakshusmathi Ghadiyaram, Muralidhara Ramachandra
  • Agents for therapy efficacy monitoring and deep tissue imaging
    Patent number: 8188116
    Abstract: Compounds and methods related to NIR molecular imaging, in-vitro and in-vivo functional imaging, therapy/efficacy monitoring, and cancer and metastatic activity imaging. Compounds and methods demonstrated pertain to the field of peripheral benzodiazepine receptor imaging, metabolic imaging, cellular respiration imaging, cellular proliferation imaging as targeted agents that incorporate signaling agents.
    Type: Grant
    Filed: July 13, 2007
    Date of Patent: May 29, 2012
    Assignee: Vanderbilt University
    Inventors: Darryl J. Bornhop, H. Charles Manning, Mingfeng Bai, Shelby K. Wyatt
  • 5-HTreceptor antagonists
    Patent number: 8188115
    Abstract: The invention relates to compounds having pharmacological activity towards the 5-HT7 receptor, and more particularly to some tetrahydroisoquinoline substituted sulfonamide compounds, to processes of preparation of such compounds, to pharmaceutical compositions comprising them, and to their use for the treatment and or prophylaxis of a disease in which 5-HT is involved, such as CNS disorders.
    Type: Grant
    Filed: August 18, 2005
    Date of Patent: May 29, 2012
    Assignee: Laboratorios Del Dr. Esteve, S.A.
    Inventors: Antoni Torrens Jover, Josep Mas Prio, Susana Yenes Minguez, Mónica Garcia Lopez, Alberto Dordal Zueras, Luz Romero Alonso, Helmut Henrich Buschmann
  • METALLOENZYME INHIBITOR COMPOUNDS
    Publication number: 20120129886
    Abstract: The instant invention describes compounds having metalloenzyme modulating activity, and methods of treating diseases, disorders or symptoms thereof mediated by such metalloenzymes.
    Type: Application
    Filed: November 10, 2011
    Publication date: May 24, 2012
    Applicant: Viamet Pharmaceuticals, Inc.
    Inventors: William J. Hoekstra, Robert J. Schotzinger, Stephen W. Rafferty
  • PHARMACEUTICAL COMPOSITIONS COMPRISING EPA AND A CARDIOVASCULAR AGENT AND METHODS OF USING THE SAME
    Publication number: 20120121698
    Abstract: The present invention relates to, inter alia, pharmaceutical compositions comprising EPA and one or more cardiovascular agents, and to therapeutic methods for treating various diseases and disorders using the same.
    Type: Application
    Filed: April 29, 2010
    Publication date: May 17, 2012
    Applicant: AMARIN PHARMA, INC.
    Inventors: Mehar Manku, Jonathan Rowe
  • INHIBITORS OF HCV NS5A
    Publication number: 20120122864
    Abstract: Provided herein are compounds, pharmaceutical compositions and combination therapies for inhibition of hepatitis C.
    Type: Application
    Filed: December 2, 2009
    Publication date: May 17, 2012
    Applicant: PRESIDIO PHARMACEUTICALS, INC.
    Inventors: Min Zhong, Leping Li
  • Biofilm-inhibiting effect and anti-infective activity of -linked aryl isoquinolines and the use thereof
    Patent number: 8173673
    Abstract: Anti-infective and biofilm-inhibiting activities of aryl isoquinoline-derivatives of the general formulae 1 to 3 are described.
    Type: Grant
    Filed: September 27, 2007
    Date of Patent: May 8, 2012
    Assignee: Julius-Maximilians-Universitaet Wuerzburg
    Inventors: Gerhard Bringmann, Tanja Gulder, Ute Hentschel, Frank Meyer, Heidrun Moll, Joachim Morschhäuser, Alicia Ponte-Sucre De Vanegas, Wilma Ziebuhr, August Stich, Reto Brun, Werner E. G. Müller, Virima Mudogo
  • 1,2,3,4-tetrahydroisoquinoline derivatives, preparation process therefor and pharmaceutical composition containing the same
    Patent number: 8173648
    Abstract: The invention provides a type of novel 1,2,3,4-tetrahydroisoquinoline derivatives with a structure of formula (I): wherein R1 represents propargyl or cyclopropylmethyl; wherein R2 represents N-ethyl-N-methylamino, 1-Pyrrolidyl, 1-Piperidinyl, or 1-Morpholinyl. The invention provides further a process for preparing said derivatives and a pharmaceutical composition containing the same. Said derivatives can be used to modulate the proteolytic process of amyloid precursor proteins (APP), and provides further novel compounds useful for treating Alzheimer's disease (AD).
    Type: Grant
    Filed: July 16, 2008
    Date of Patent: May 8, 2012
    Assignee: National Defense Medical Center
    Inventors: Ming-Kuan Hu, Yung-Feng Liao
  • Crystalline Pharmaceutical and Methods of Preparation and Use Thereof
    Publication number: 20120107404
    Abstract: Novel crystalline polymorphic forms, Forms A, B, C, D, and E of a compound of Formula I, which has been found to be a potent inhibitor of LFA-1, are disclosed. Methods of preparation and uses thereof in the treatment of LFA-1 mediated diseases are also disclosed in this invention.
    Type: Application
    Filed: November 4, 2011
    Publication date: May 3, 2012
    Applicant: SARcode Bioscience Inc.
    Inventors: John Burnier, Thomas Gadek, Frederic Naud
  • PROTEASE INHIBITORS
    Publication number: 20120108529
    Abstract: Compounds useful as protease inhibitors are provided, as are methods of use and preparation of such compounds and compositions containing such compounds. In one embodiment, the compounds are useful for inhibiting HIV protease enzymes, and are therefore useful in slowing the proliferation of HIV.
    Type: Application
    Filed: May 14, 2010
    Publication date: May 3, 2012
    Inventors: Robert R. Webb, II, Mitchell W. Mutz, Kenneth J. Barr
  • Compositions and methods for treatment of eye disorders
    Patent number: 8168655
    Abstract: The present invention provides compounds and methods for the treatment of LFA-1 mediated diseases. In particular, LFA-1 antagonists are described herein and these antagonists are used in the treatment of LFA-1 mediated diseases. One aspect of the invention provides for diagnosis of an LFA-1 mediated disease and administration of a LFA-1 antagonist, after the patient is diagnosed with a LFA-1 mediated disease. In some embodiments, the LFA-1 mediated diseases treated are dry eye disorders. Also provided herein are methods for identifying compounds which are LFA-1 antagonists.
    Type: Grant
    Filed: May 17, 2006
    Date of Patent: May 1, 2012
    Assignee: SARcode Bioscience Inc.
    Inventors: Thomas Gadek, John Burnier
  • SUBSTITUTED ISOQUINOLINE DERIVATIVES, PHARMACEUTICAL COMPOSITIONS, AND METHODS OF USE AS BETA-SECRETASE INHIBITORS
    Publication number: 20120101125
    Abstract: The present invention is directed to substituted isoquinoline derivatives, pharmaceutically acceptable salts thereof, and tautomers of such compounds or salts, that inhibit ?-site amyloid precursor protein-cleaving enzyme (BACE) and that may be useful in the treatment of diseases in which BACE is involved, such as Alzheimer's disease. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the treatment of such diseases in which BACE is involved.
    Type: Application
    Filed: August 22, 2011
    Publication date: April 26, 2012
    Applicant: HIGH POINT PHARMACEUTICALS, LLC
    Inventors: Adnan M. M. Mjalli, Bapu Gaddam, Devi Reddy Gohimukkula, Dharma Rao Polisetti, Hassan El Abdellaoui, Mohan Rao, Pingzhen Wang, Robert Carl Andrews, Rongyuan Xie, Tan Ren
  • ARYL SULFONAMIDES
    Publication number: 20120101097
    Abstract: The present invention relates to compounds that modulate various chemokine receptors. These compounds are useful for treating inflammatory and immune diseases.
    Type: Application
    Filed: March 10, 2011
    Publication date: April 26, 2012
    Inventors: Solomon Ungashe, John Jessen Wright, Andrew Pennell
  • ARYL SUBSTITUTED CARBOXAMIDE DERIVATIVES AS CALCIUM OR SODIUM CHANNEL BLOCKERS
    Publication number: 20120101105
    Abstract: The present invention relates to aryl substituted carboxamide derivatives of formula (I) or a pharmaceutically acceptable salt thereof, which have blocking activities of T-type calcium channels or voltage gated sodium channels as the tetrodotoxin-sensitive (TTX-S) blockers such as Nav1.3 and Nav1.7, and which are useful in the treatment or prevention of disorders and diseases in which T-type calcium channels or voltage gated sodium channels are involved. The invention also relates to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which T-type calcium channels or voltage gated sodium channels are involved.
    Type: Application
    Filed: May 31, 2010
    Publication date: April 26, 2012
    Inventors: Tadashi Inoue, Shuzo Watanabe, Tatsuya Yamagishi, Yoshimasa Arano, Mikio Morita, Kaoru Shimada
  • IMIDAZOLE DERIVATIVES AND THEIR USE AS MODULATORS OF CYCLIN DEPENDENT KINASES
    Publication number: 20120101064
    Abstract: The invention provides compounds of the formula (I): and salts, tautomers, solvates and N-oxides thereof; wherein Q is CH or N; X is N, N+—O? or CR3; Y is N, N+—O? or CR3a; R1 and R2 are independently selected from hydrogen and various substituents as defined in the claims; or R1 and R2 together with the atoms to which they are attached, link to form an optionally substituted carbocyclic or heterocyclic aromatic or non-aromatic ring of 4 to 7 members; R3 is selected from hydrogen and various substituents; and R3a is selected from hydrogen and various substituents as defined in the claims. Also provided are pharmaceutical compositions containing the compounds of formula (I), processes for making the compounds and the medical uses of the compounds. The compounds of formula (I) have activity as inhibitors of CDK kinases and are useful in the treatment of inter alia proliferative diseases such as cancers.
    Type: Application
    Filed: April 30, 2010
    Publication date: April 26, 2012
    Applicants: Astex Therapeutics Limited, Novartis AG
    Inventors: Steven Howard, Paul Neil Mortenson, Steven Douglas Hiscock, Alison Jo-Anne Woolford, Andrew James Woodhead, Gianni Chessari, Marc O'reilly, Miles Stuart Congreve, Claudio Dagostin, Young Shin Cho, Fan Yang, Christine Hiu-Tung Chen, Christopher Thomas Brain, Bharat Lagu, Yaping Wang, Sunkyu Kim, John Grialdes, Michael Joseph Luzzio, Lawrence Blas Perez
  • S1P1 AGONISTS COMPRISING A BICYCLIC N-CONTAINING RING
    Publication number: 20120101083
    Abstract: The present invention relates to novel compounds of formula (I) having S1P1 agonist activity, processes for their preparation, pharmaceutical compositions containing them and their use in the treatment of various disorders.
    Type: Application
    Filed: June 17, 2010
    Publication date: April 26, 2012
    Applicant: GLAXO GROUP LIMITED
    Inventors: James Matthew Bailey, Rino Antonio Bit, Emmanuel Hubert Demont, Lee Andrew Harrison, Katherine Louise Jones, Christian Alan Paul Smethurst, Jason Witherington
  • Hepatitis C virus inhibitors
    Patent number: 8163921
    Abstract: Hepatitis C virus inhibitors having the general formula are disclosed. Compositions comprising the compounds and methods for using the compounds to inhibit HCV are also disclosed.
    Type: Grant
    Filed: April 6, 2009
    Date of Patent: April 24, 2012
    Assignee: Bristol-Myers Squibb Company
    Inventors: Ny Sin, Brian Lee Venables, Paul Michael Scola, Alan Xiangdong Wang
  • THIAZOLE OR THIADIZALOE DERIVATIVES FOR USE AS SPHINGOSINE 1-PHOSPHATE 1 (S1P1) RECEPTOR AGONISTS
    Publication number: 20120094979
    Abstract: Thiazole or thiadizaloe derivatives of formula (I) or pharmaceutical salts thereof having pharmacological activity, processes for their preparation, pharmaceutical compositions containing them and their uses in the treatment of various disorders mediated by S1P1 receptor are disclosed.
    Type: Application
    Filed: June 17, 2010
    Publication date: April 19, 2012
    Applicant: Glaxo Wellcome House
    Inventors: James Matthew Bailey, Emmanuel Hubert Demont, Xichen Lin, Feng Ren, Christian Alan Paul Smethurst
  • SMOOTHENED RECEPTOR MODULATORS
    Publication number: 20120094974
    Abstract: The present invention relates, in general, to the Smoothened receptor and, in particular, to a method of modulating Smoothened receptor activity and to compounds and compositions suitable for use in such a method.
    Type: Application
    Filed: June 16, 2009
    Publication date: April 19, 2012
    Inventors: Wei Chen, Lawrence Barak, H. Kim Lyerly, Jiangbo Wang
  • QUINOLINES AS INHIBITORS OF FARNESYL PYROPHOSPHATE SYNTHASE
    Publication number: 20120094958
    Abstract: The invention relates to a compound of formula (I) wherein the substituents are as described in the specification, which are useful as farnesyl pyrophosphate synthase modulators, e.g. in the treatment of proliferative diseases, to methods of manufacturing such compounds and to intermediates thereof.
    Type: Application
    Filed: February 26, 2009
    Publication date: April 19, 2012
    Applicant: NOVARTIS AG
    Inventors: Rene Amstutz, Guido Bold, Simona Cotesta, Wolfgang Jahnke, Andreas Marzinzik, Juliane Constanze Desiree Hartwieg, Silvio Ofner, Frédérik Stauffer, Johann Zimmermann
  • PHARMACEUTICAL COMPOSITIONS COMPRISING EPA AND A CARDIOVASCULAR AGENT AND METHODS OF USING THE SAME
    Publication number: 20120093922
    Abstract: The present invention relates to, inter alia, pharmaceutical compositions comprising EPA and one or more cardiovascular agents, and to therapeutic methods for treating various diseases and disorders using the same.
    Type: Application
    Filed: April 29, 2010
    Publication date: April 19, 2012
    Applicant: AMARIN CORPORATION PLC
    Inventors: Mehar Manku, Jonathan Rowe
  • TRICYCLIC DELTA-OPIOID MODULATORS
    Publication number: 20120095010
    Abstract: The invention is directed to delta opioid receptor modulators. More specifically, the invention relates to tricyclic ?-opioid modulators. Pharmaceutical and veterinary compositions and methods of treating mild to severe pain and various diseases using compounds of the invention are also described.
    Type: Application
    Filed: December 22, 2011
    Publication date: April 19, 2012
    Inventors: John R. Carson, Ellen Codd, Christine M. Razler, Andrea Works, Mark McDonnell, James J. McNally
  • CYCLOPENTA[C]PYRROLE-2-CARBOXYLATE DERIVATIVES, PREPARATION THEREOF AND THERAPEUTIC USE THEREOF
    Publication number: 20120095040
    Abstract: The invention relates to compounds of the general formula (I) where: R2 is a hydrogen or fluorine atom or a hydroxyl, cyano, trifluoromethyl, C1-6-alkyl, C1-6-alkoxy, or NR8R9 group; m, n, o and p independently are a number from 0 to 3; A is a covalent bond, an oxygen atom, a C1-6-alkylene group or a —O—C1-6-alkylene group in which the end that is an oxygen atom is bonded to the R1 group while the end that is an alkylene group is bonded to the carbon of the bicyclic compound; R1 is an optionally substituted aryl or heteroaryl group; R3 is a hydrogen or fluorine atom or a C1-6-alkyl or trifluoromethyl group; R4 is an optionally substituted 5-membered heterocyclic compound; wherein the compounds can be in the state of a base or an acid addition salt. The invention can be used in therapeutics.
    Type: Application
    Filed: May 11, 2010
    Publication date: April 19, 2012
    Applicant: SANOFI
    Inventors: Ahmed Abouabdellah, Luc Even, Aude Fayol, Julien Vache, Philippe Yauche
  • FIVE-MEMBERED HETEROCYCLES USEFUL AS SERINE PROTEASE INHIBITORS
    Publication number: 20120088758
    Abstract: The present invention provides a method for treating a thrombotic or an inflammatory disorder administering to a patient in need thereof a therapeutically effective amount of at least one compound of Formula (I) or Formula (V): or a stereoisomer or pharmaceutically acceptable salt or solvate form thereof, wherein the variables A, L, Z, R3, R4, R6, R11, X1, X2, and X3 are as defined herein. The compounds of Formula (I) are useful as selective inhibitors of serine protease enzymes of the coagulation cascade and/or contact activation system; for example thrombin, factor Xa, factor XIa, factor IXa, factor VIIa and/or plasma kallikrein. In particular, it relates to compounds that are selective factor XIa inhibitors. This invention also provides compounds within the scope of Formula I and relates to pharmaceutical compositions comprising these compounds.
    Type: Application
    Filed: December 15, 2011
    Publication date: April 12, 2012
    Inventors: Jon J. Hangeland, Mimi L. Quan, Joanne M. Smallheer, Gregory S. Bisacchi, James R. Corte, Todd J. Friends, Zhong Sun, Karen A. Rossi, Cullen L. Cavallaro
  • PHENALKYLAMINE DERIVATIVES, PHARMACEUTICAL COMPOSITIONS CONTAINING THEM, AND THEIR USE IN THERAPY
    Publication number: 20120088790
    Abstract: The present invention relates to phenalkylamine derivatives of the formula (I) or (II) or a physiologically tolerated salt thereof. The invention relates to pharmaceutical compositions comprising such phenalkylamine derivatives, and the use of such phenalkylamine derivatives for therapeutic purposes. The phenalkylamine derivatives are GlyT1 inhibitors.
    Type: Application
    Filed: August 10, 2011
    Publication date: April 12, 2012
    Applicants: Abbott GmbH & Co. KG, Abbott Laboratories
    Inventors: Frauke Pohlki, Udo Lange, Wilhelm Amberg, Michael Ochse, Berthold Behl, Charles W. Hutchins, Wilfried Hornberger, Mario Mezler
  • Compositions useful as inhibitors of voltage-gated sodium channels
    Patent number: 8153655
    Abstract: The present invention relates to compounds useful as inhibitors of voltage-gated sodium channels. The invention also provides pharmaceutically acceptable compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various disorders.
    Type: Grant
    Filed: September 10, 2009
    Date of Patent: April 10, 2012
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: Jesus Gonzalez, III, Andreas Termin, Esther Martinborough, Nicole Zimmermann
  • 6-and 7-amino isoquinoline compounds and methods for making and using the same
    Patent number: 8153654
    Abstract: 6- and 7-amino isoquinoline compounds are provided that influence, inhibit or reduce the action of a kinase. Pharmaceutical compositions including therapeutically effective amounts of the 6- and 7-aminoisoquinoline compounds and pharmaceutically acceptable carriers are also provided. Various methods using the compounds and/or compositions to affect disease states or conditions such as cancer, obesity and glaucoma are also provided.
    Type: Grant
    Filed: January 17, 2008
    Date of Patent: April 10, 2012
    Assignee: Aerie Pharmaceuticals, Inc.
    Inventors: Mitchell A. deLong, Jill Marie Sturdivant, Geoffrey Richard Heintzelman, Susan M. Royalty
  • Sulfonamides as TRPM8 modulators
    Patent number: 8148422
    Abstract: Disclosed are compounds, compositions and methods for treating various diseases, syndromes, conditions and disorders, including pain. Such compounds are represented by Formula (I) and Formula (II) as follows: wherein Y, R1, R2, R3, R4, RA, and RB are defined herein.
    Type: Grant
    Filed: December 15, 2009
    Date of Patent: April 3, 2012
    Assignee: Janssen Pharmaceutica, NV
    Inventors: Mark J. Macielag, James J. McNally
  • 5-HT7 receptor antagonists
    Patent number: 8148397
    Abstract: The invention relates to compounds having pharmacological activity towards the 5-HT7 receptor, and more particularly to some tetrahydroisoquinoline propyl sulfonamide compounds, to processes of preparation of such compounds, to pharmaceutical compositions comprising them, and to their use for the treatment and or prophylaxis of a disease in which 5-HT is involved, such as CNS disorders.
    Type: Grant
    Filed: August 18, 2005
    Date of Patent: April 3, 2012
    Assignee: Laboratorios Del Dr. Esteve, S.A.
    Inventors: Antoni Torrens Jover, Josep Mas Prio, Susana Yenes Minguez, Monica Garcia Lopez, Alberto Dordal Zueras, Luz Romero Alonso, Helmut Henrich Buschmann
  • Compounds for the Treatment of Metabolic Disorders
    Publication number: 20120077793
    Abstract: The present invention is directed to therapeutic compounds which have activity as agonists of GPR119 and are useful for the treatment of metabolic disorders including type II diabetes.
    Type: Application
    Filed: March 12, 2010
    Publication date: March 29, 2012
    Applicant: PROSIDION LIMITED
    Inventors: Oscar Barba, Peter Timothy Fry, Matthew Colin Thor Fyfe, William Gattrell, Revathy Perpetua Jeevaratnam, Thomas Martin Krulle, Martin James Procter, Colin Peter Sambrook-Smith, Karen Lesley Schofield, Donald Smyth, Alan John William Stewart, David French Stonehouse, Simon Andrew Swain
  • METHOD AND SYSTEM FOR EFFECTING CHANGES IN PIGMENTED TISSUE
    Publication number: 20120076848
    Abstract: Methods and systems are described for a rapid and sustainable change in the pigment melanin content of melanocytes of the iris stroma, thereby to change the color of the eye. Also described are nanoparticle compositions for lightening the pigmented tissues or treating a pigmented tissue related disease.
    Type: Application
    Filed: July 21, 2010
    Publication date: March 29, 2012
    Inventor: Kambiz Thomas Moazed
  • Use of triazolopyrimidine derivatives as microbicides
    Patent number: 8143275
    Abstract: Use of compounds of the formula (I) in which R1, R2, R3 and R4 are as defined in the description for protecting engineered materials.
    Type: Grant
    Filed: December 31, 2010
    Date of Patent: March 27, 2012
    Assignee: LANXESS Deutschland GmbH
    Inventors: Rainer Bruns, Martin Kugler, Thomas Jaetsch, Hans-Ludwig Elbe, Dietmar Kuhnt, Olaf Gebauer, Heiko Rieck
  • INHIBITOR COMPOUNDS OF 11-BETA-HYDROXYSTEROID DEHYDROGENASE TYPE 1
    Publication number: 20120071466
    Abstract: The compounds of formula (I) are derived from perhydroquinoline and perhydroisoquinoline and are useful as active pharmaceutical ingredients for the prophylaxis or treatment of diseases caused by 11-beta-hydroxysteroid dehydrogenase type I (11-beta-HSD1) enzyme-associated disorders, such as glaucoma, elevated ocular pressure, metabolic disorders, obesity, metabolic syndrome, dyslipidemia, hypertension, diabetes, atherosclerosis, Cushing's syndrome, psoriasis, rheumatoid arthritis, cognitive disorders, Alzheimer's disease or neurodegeneration.
    Type: Application
    Filed: June 4, 2010
    Publication date: March 22, 2012
    Inventors: Juan Lorenzo Catena Ruiz, Carme Serra Comas, Oscar Rey Puiggros, Albert Antolin Hernandez, Esther Monlleomas
  • PYRAZOLE OXADIAZOLE DERIVATIVES AS S1P1 AGONISTS
    Publication number: 20120071460
    Abstract: The present invention relates to pyrazole oxadiazoles derivatives of Formula (I), and their use for treating multiple sclerosis and other diseases, wherein R1, R2 and R3 are as defined in the description.
    Type: Application
    Filed: June 7, 2010
    Publication date: March 22, 2012
    Applicant: MERCK SERONO SA
    Inventors: Anna Quattropani, Charles Baker-Glenn, Wesley Blackaby, Chris Knight
  • INHIBITORS OF BACTERIAL PLASMINOGEN ACTIVATORS
    Publication number: 20120064062
    Abstract: Organic compounds showing the ability to inhibit bacterial omptin proteases, specifically Yersinia pestis plasminogen activator (Pla) are disclosed. The disclosed Y. pestis plasminogen activator inhibitor compounds are useful for treating, preventing, or reducing the spread of infections by Y. pestis.
    Type: Application
    Filed: September 13, 2011
    Publication date: March 15, 2012
    Inventors: Jon D. Goguen, Daniel Aiello, Donald T. Moir, Bing Li
  • SUBSTITUTED HETEROCYCLIC DERIVATIVES AND THEIR PHARMACEUTICAL USE AND COMPOSITIONS
    Publication number: 20120065188
    Abstract: Compounds of the general Formula I, wherein X1, X2, X3, X4, X5, X6, X7, R1, R2, R4, R5, R6, R7, R8, R9, R10, Y1, n, m, p and q are defined as above, their preparation and their use as antimicrobial agents.
    Type: Application
    Filed: November 22, 2011
    Publication date: March 15, 2012
    Inventors: Steven Joseph Brickner, Jinshan Michael Chen, Zhengong Bryan Li, Anthony Marfat, Mark Joseph Mitton-Fry, Michael A. Plotkin, Usa Datta Reilly, Chakrapani Subramanyam, Zhijun Zhang, Shaughnessy Robinson
  • ANTIMICROBIAL AGENTS
    Publication number: 20120059026
    Abstract: The invention provides a compound of formula (I): or a salt or prodrug thereof, wherein Y, W, Z, Z1, Z2, Z3, Z4, and R1-R12 have any of the values described in the specification, as well as compositions comprising a compound of formula (I). The compounds are useful as antibacterial agents.
    Type: Application
    Filed: April 30, 2010
    Publication date: March 8, 2012
    Applicants: University of Medicine and Dentistry of New Jersey, Rutgers, The State University of New Jersey
    Inventors: Edmond J. LaVoie, Daniel S. Pilch, Ajit Parhi, Malvika Kaul
  • 1,2,3,4-TETRAHYDROISOQUINOLINE DERIVATIVES EFFECTIVE AS ANTIGLIOMA AGENTS, METHODS OF MAKING, AND THEIR USE
    Publication number: 20120059032
    Abstract: Disclosed are tetrahydroisoquinoline-derivative compounds effective for killing cancer cells, shrinking tumor size, and treating cancer.
    Type: Application
    Filed: March 7, 2011
    Publication date: March 8, 2012
    Applicant: University of Tennessee Research Foundation
    Inventors: Renukadevi Patil, Shivaputra A. Patil, Duane D. Miller, Charles Ryan Yates, Eldon E. Geisert
  • Fungicide hydroximoyl-tetrazole derivatives
    Patent number: 8129415
    Abstract: The present invention relates to hydroximoyl-tetrazole derivatives of formula (I) wherein T represent a tetrazolyl substituent, A represents a carbo- or heterocycle, L1 and L2 represent various linking groups and Q represents a 6-membered heterocycle, their process of preparation, their use as fungicide active agents, particularly in the form of fungicide compositions, and methods for the control of phytopathogenic fungi, notably of plants, using these compounds or compositions.
    Type: Grant
    Filed: July 12, 2007
    Date of Patent: March 6, 2012
    Assignee: Bayer Cropscience AG
    Inventors: Isabelle Christian, Marie-Claire Grosjean-Cournoyer, Pierre Hutin, Philippe Rinolfi, Arounarith Tuch, Jacky Vidal
  • 3-SUBSTITUTED PROPANAMINE COMPOUNDS
    Publication number: 20120046312
    Abstract: Racemic or enantiomerically enriched 3-substituted propanamine compounds represented by the following structural formula (I): or a pharmaceutically acceptable salt thereof are disclosed. Pharmaceutical compositions containing the subject compounds are also disclosed. The subject compounds are useful for the treatment of diseases of the central nervous system, such as depression, anxiety and pain disorders.
    Type: Application
    Filed: October 19, 2011
    Publication date: February 23, 2012
    Inventors: Chun-Eung Park, Kyung-Hyun Min, Yong-Je Shin, Yu-Jin Shin, Hae-Jeong Yoon, Won Kim, Eun-Ju Ryu, Coo-Min Chung, Hui-Ho Kim
  • COMPOUNDS FOR THE TREATMENT OF PROLIFERATIVE DISORDERS
    Publication number: 20120040937
    Abstract: The invention relates to compounds of structural formula (I): or a pharmaceutically acceptable salt, solvate, clathrate, and prodrug thereof, wherein Ra, Rb, and R2 are defined herein. These compounds inhibit tubulin polymerization and/or target vasculature and are useful for treating proliferative disorders, such as cancer.
    Type: Application
    Filed: October 7, 2011
    Publication date: February 16, 2012
    Inventors: Lijun Sun, Jun Jiang, Christopher Borella, Shoujun Chen, Keizo Koya
  • CARBONYLAMINO-DERIVATIVES AS NOVEL INHIBITORS OF HISTONE DEACETYLASE
    Publication number: 20120041001
    Abstract: This invention comprises the novel compounds of formula (I) wherein n, m, t, R1, R2, R3, R4, R5, L, Q, X, Y and have defined meanings, having histone deacetylase inhibiting enzymatic activity; their preparation, compositions containing them and their use as a medicine.
    Type: Application
    Filed: October 24, 2011
    Publication date: February 16, 2012
    Applicant: Janssen Pharmaceutica, NV
    Inventors: Kristof Van Emelen, Marc Gustaaf Celine Verdonck, Sven Franciscus Anna Van Brandt, Leo Jacobus Jozef Backx
  • CYCLIC COMPOUND HAVING SUBSTITUTED PHENYL GROUP
    Publication number: 20120040936
    Abstract: Low molecular weight compound exhibiting an osteogenesis-promoting action having the general formula (I) or a pharmacologically acceptable salt thereof:
    Type: Application
    Filed: October 5, 2011
    Publication date: February 16, 2012
    Applicant: DAIICHI SANKYO COMPANY, LIMITED
    Inventors: Osamu Kanno, Katsuyoshi Nakajima, Kazumasa Aoki, Ryoichi Tanaka, Shimpei Hirano, Kiyoshi Oizumi, Satoru Naito
  • SUBSTITUTED ISOQUINOLINE DERIVATIVE
    Publication number: 20120035159
    Abstract: The present invention provides an isoquinoline-6-sulfonamide derivative that is useful as a novel pharmaceutical agent. The present invention provides an isoquinoline-6-sulfonamide derivative represented by Formula (1), a salt thereof, or a solvate of the derivative or the salt: wherein X and Y each independently represent a direct bond, NH, CH?CH, O, or S; R1 and R2 each independently represent a hydrogen atom, a halogen atom, a cyano group, an alkyl group, or the like; R3 and R4 each independently represent a hydrogen atom, an alkyl group, or the like, or R3 and R4 together form an alkylene group or an alkenylene group, which may be bridged between two carbon atoms to an arbitrary position; and l, m, and n represent an integer number of 1 to 4.
    Type: Application
    Filed: June 18, 2010
    Publication date: February 9, 2012
    Applicant: D. WESTERN THERAPEUTICS INSTITUTE, INC
    Inventors: Hiroyoshi Hidaka, Kouichi Takahashi, Yoshihiro Inoue, Kengo Sumi, Ryohei Nakamura
  • S1P Receptors Modulators
    Publication number: 20120034270
    Abstract: The invention relates to novel compounds that have S1P receptor modulating activity and, preferably, apoptotic activity and/or anti proliferative activity against cancer cells and other cell types. Further, the invention relates to a pharmaceutical comprising at least one compound of the invention for the treatment of diseases and/or conditions caused by or associated with in-appropriate S1P receptor modulating activity or expression, for example, cancer. A further aspect of the invention relates to the use of a pharmaceutical comprising at least one compound of the invention for the manufacture of a medicament for the treatment of diseases and/or conditions caused by or associated with inappropriate S1P receptor modulating activity or expression such as cancer.
    Type: Application
    Filed: October 16, 2009
    Publication date: February 9, 2012
    Applicant: Akaal Pharma Pty Ltd
    Inventors: Damian W. Grobelny, Gurmit S. Gill
  • MODULATORS OF ATP-BINDING CASSETTE TRANSPORTERS
    Publication number: 20120035179
    Abstract: The present invention provides compounds of Formula I useful as modulators of ABC transporter activity, or a pharmaceutically acceptable salt thereof, wherein RB, n, B, RC, RD, RE, A, and Z are described generally and in classes and subclasses below. The present invention also provides pharmaceutical compositions, methods and kits associated with Formula I, useful for as modulators, and for the treatments of disease and disease conditions associated with ABC transporter proteins.
    Type: Application
    Filed: March 9, 2011
    Publication date: February 9, 2012
    Inventors: Sara S. Hadida-Ruah, Mark Miller, Ashvani Singh, Matthew Hamilton, Peter D.J. Grootenhuis
  • Modulators of Cellular Adhesion
    Publication number: 20120035154
    Abstract: The present invention provides compounds having formula (I): and pharmaceutically acceptable derivatives thereof, wherein R1-R4, n, p, A, B, D, E, L and AR1 are as described generally and in classes and subclasses herein, and additionally provides pharmaceutical compositions thereof, and methods for the use thereof for the treatment of disorders mediated by the CD11/CD18 family of cellular adhesion molecules (e.g., LFA-1).
    Type: Application
    Filed: September 1, 2011
    Publication date: February 9, 2012
    Applicant: SARcode Bioscience, Inc.
    Inventors: Wang SHEN, Kenneth BARR, Johan D. OSLOB, Min ZHONG
  • INDOLE-2-CARBOXAMIDE DEIVATIVE
    Publication number: 20120035155
    Abstract: To provide an indole compound having a human QRFP receptor antagonistic activity and useful as a preventive or a remedy for various disorders. A compound of a formula (I) or a pharmaceutically-acceptable salt thereof is provided: [wherein, R1 represents a hydrogen atom, a halogen, a C1-6 alkyl, etc,; R2 represents a C1-6 alkyl, or a halo-C1-6 alkyl; R3 represents a hydrogen atom, a C1-6 alkyl, etc.; R4 represents a hydrogen atom, a C1-6 alkyl, a halo-C1-6 alkyl, etc.; or R3 and R4, taken together with the nitrogen atom to which they bond, form a 3- to 6-membered aliphatic nitrogen-containing hetero ring; or R3 and Y3, taken together, form —CH2—CH2—; Y1 and Y2 are both hydrogen atoms; or Y1 and Y2, taken together, form —CH2—CH2—; and Y3 represents a hydrogen atom; or Y3 and R3, taken together, form —CH2—CH2—].
    Type: Application
    Filed: April 17, 2010
    Publication date: February 9, 2012
    Applicant: MSD K.K.
    Inventors: Yuji Haga, Sayaka Mizutani, Nagaaki Sato
  • CHEMICAL COMPOUNDS
    Publication number: 20120035164
    Abstract: The invention is directed to novel indole carboxamide derivatives. Specifically, the invention is directed to compounds according to formula I: where R1, R2, R3, U and V are defined below and to pharmaceutically acceptable salts thereof. The compounds of the invention are inhibitors of IKK2 and can be useful in the treatment of disorders associated with inappropriate IKK2 (also known as IKK?) activity, such as rheumatoid arthritis, asthma, and COPD (chronic obstructive pulmonary disease). Accordingly, the invention is further directed to pharmaceutical compositions comprising a compound of the invention. The invention is still further directed to methods of inhibiting IKK2 activity and treatment of disorders associated therewith using a compound of the invention or a pharmaceutical composition comprising a compound of the invention.
    Type: Application
    Filed: October 14, 2011
    Publication date: February 9, 2012
    Inventors: Jianghe DENG, Jeffrey K. KERNS, Qi JIN, Guoliang LIN, Xichen LIN, Michael LINDENMUTH, Christopher NEIPP, Hong NIE, Sonia M. THOMAS, Katherine L. WIDDOWSON
  • 2,3-DIHYDROBENZO(1,4) DIOXIN-2-YLMETHYL DERIVATIVES AS ALPHA2C ANTAGONISTS FOR USE IN THE TREATMENT OF PERIPHERIC AND CENTRAL NERVOUS SYSTEME DISEASES
    Publication number: 20120035210
    Abstract: Compounds of formula I wherein X, Z, R1-R4, and m are as defined in the claims, exhibit alpha2C antagonistic activity, and are thus useful as alpha2C antagonists. Methods for the treatment of diseases and conditions of the peripheric system and the central nervous system are also disclosed.
    Type: Application
    Filed: July 18, 2008
    Publication date: February 9, 2012
    Inventors: David Din Belle, Patrik Holm, Arto Karljalainen, Arto Tolvanen, Gerd Wohlfahrt, Petteri Rummakko