The Additional Polycyclo Ring System Is A Bicyclo Ring System Having Nitrogen As The Only Ring Hetero Atom [e.g., 5-(indolyl-3-methylene)- Hydantoin, Etc.] Patents (Class 548/312.1)
  • Publication number: 20130264554
    Abstract: An organic electroluminescent device comprising: a pair of electrodes comprising an anode and a cathode, and one or more layers of organic compound arranged between the pair of electrodes, wherein the organic compound layer, or one or more of the organic compound layers, comprises a compound represented by a substituted imidazole. The substituents on the imidazole ring may be selected from a range of suitable substituents, including: substituted or unsubstituted aryl groups, substituted or unsubstituted heterocyclic groups, substituted or unsubstituted alkyl groups or cyano groups. In various aspects of the invention, at least one of the substituent groups may be a substituted or unsubstituted imidazole or thiophene group.
    Type: Application
    Filed: October 21, 2011
    Publication date: October 10, 2013
    Inventors: James Matthew MacDonald, Kazunori Ueno, Karl Peter Weber, Tadahiko Hirai, Juo-Hao Li
  • Publication number: 20130263390
    Abstract: The invention relates to 4-aminoindole derivatives of formula (I), and the addition salts thereof, mesomers thereof, isomers thereof and solvates thereof: and to their use for the oxidation dyeing of keratin fibres, and in particular of human keratin fibres such as the hair. The present invention makes it possible to achieve dark shades, natural shades and dark natural shades. The present invention also makes it possible to obtain powerful, chromatic, aesthetic, sparingly selective coloration of keratin fibres in varied shades, which is resistant to the various attacking factors to which the hair may be subjected. In particular, when the 4-aminoindole derivatives are combined with one or more heterocyclic oxidation bases, they make it possible to obtain a wide range of colours and coloration of keratin fibres that shows good chromaticity and good selectivity.
    Type: Application
    Filed: December 14, 2011
    Publication date: October 10, 2013
    Applicant: L'OREAL
    Inventors: Aziz Fadli, Fatima Makhlouf
  • Patent number: 8541572
    Abstract: This invention relates to compounds of the Formula (I): (Chemical formula should be inserted here as it appears on abstract in paper form) (I) or a pharmaceutically acceptable salt, solvate or isomer thereof, which can be useful for the treatment of diseases or conditions mediated by MMPs, ADAMs, TACE, aggrecanase, TNF—or combinations thereof.
    Type: Grant
    Filed: November 9, 2009
    Date of Patent: September 24, 2013
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Joseph A. Kozlowski, Wensheng Yu, Michael K. C. Wong, Seong Heon Kim, Ling Tong, Brian J. Lavey, Bandarpalle B. Shankar, De-Yi Yang, Robert Feltz, Aneta Maria Kosinski, Guowei Zhou, Razia K. Rizvi, Chaoyang Dai, Luke Fire, Vinay Girijavallabhan, Dansu Li, Janeta Popovici-Muller, Judson E. Richard, Kristin E. Rosner, M. Arshad Siddiqui, Liping Yang
  • Publication number: 20130225617
    Abstract: Compounds of the invention are ligands of the CRTH2 receptor, useful inter alia for treatment of inflammatory conditions.
    Type: Application
    Filed: January 31, 2013
    Publication date: August 29, 2013
    Applicant: PULMAGEN THERAPEUTICS (ASTHMA) LIMITED
    Inventor: PULMAGEN THERAPEUTICS (ASTHMA) LIMITED
  • Publication number: 20130210880
    Abstract: The present invention relates to isoindoline derivatives of the formula (I) or a physiologically tolerated salt thereof. The present invention also relates to pharmaceutical compositions comprising such isoindoline derivatives, and the use of such isoindoline derivatives for therapeutic purposes.
    Type: Application
    Filed: February 11, 2013
    Publication date: August 15, 2013
    Applicants: AbbVie Inc., AbbVie Deutschland GmbH & Co. KG
    Inventors: AbbVie Deutschland GmbH & Co. KG, AbbVie Inc.
  • Publication number: 20130211079
    Abstract: MDM2 and MDM4 proteins prevent apoptosis of cancer cells by negatively regulating the transcription factor p53. Compounds according to Formula I are selective antagonists of MDM2 and MDM4 proteins, disrupting the p53/MDM2 and p53/MDM4 complex. These compounds therefore are candidate therapeutics for treating cancer as well as other cell proliferative disease states.
    Type: Application
    Filed: March 15, 2013
    Publication date: August 15, 2013
    Inventor: Alexander DOEMLING
  • Patent number: 8507521
    Abstract: The present invention relates to a heterocyclic derivative of formula (I) wherein the variables are as defined in the specification, or to a pharmaceutically acceptable salt or solvate thereof. The present invention further relates to pharmaceutical compositions comprising said heterocyclic derivatives and to their use in therapy, for instance in the treatment or prevention of disorders mediated by glutamate dysfunction, such as schizophrenia and generalised anxiety disorder.
    Type: Grant
    Filed: November 2, 2010
    Date of Patent: August 13, 2013
    Assignee: Merck Sharp + Dohme B.V.
    Inventors: Julia Adam, Jonathan Gillespie, Steven Laats, John Kinnaird Ferguson MacLean, Duncan Robert McArthur
  • Patent number: 8501747
    Abstract: In its many embodiments, the present invention provides a novel class of biaryl compounds as inhibitors of ÿ2C adrenergic receptor agonists, methods of preparing such compounds, pharmaceutical compositions containing one or more such compounds, methods of preparing pharmaceutical formulations comprising one or more such compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more conditions associated with the ÿ2C adrenergic receptors using such compounds or pharmaceutical compositions.
    Type: Grant
    Filed: February 11, 2008
    Date of Patent: August 6, 2013
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Manuel de lera Ruiz, Kevin D. McCormick, Christopher W. Boyce, Robert G. Aslanian, Younong Yu, Pietro Mangiaracina, Junying Zheng, Michael Y. Berlin, Stephanie Louise Ciesla, Chia-Yu Huang, Bo Liang
  • Publication number: 20130196971
    Abstract: This invention relates to the use of imidazole, triazole, and tetrazole derivatives for the modulation, notably the inhibition of the activity or function of fatty acid synthase (FAS). Suitably, the present invention relates to the use of imidazoles, triazoles, and tetrazoles in the treatment of cancer.
    Type: Application
    Filed: September 15, 2011
    Publication date: August 1, 2013
    Inventors: Christopher Joseph Aquino, Dennis Heyer, Terence John Kiesow, David Lee Musso, Cynthia A. Parrish
  • Patent number: 8492556
    Abstract: The present invention relates to novel 2,5-dioxoimidazolidin-1-yl-3-phenylurea derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of the N-formyl peptide receptor like-1 (FPRL-1) receptor.
    Type: Grant
    Filed: November 9, 2012
    Date of Patent: July 23, 2013
    Assignee: Allergan, Inc.
    Inventors: Richard L. Beard, Vidyasagar Vuligonda, Thong Vu, John E. Donello, Veena Viswanath, Michael E. Garst
  • Patent number: 8487113
    Abstract: The invention deals with a preparation method of salts of 5-chloro-4-(2-imidazolin-2-yl-amino)-2,1,3-benzothiadiazole (tizanidine) of formula I, especially tizanidine hydrochloride, comprising preparation of a salt of tizanidine of formula I and a carboxylic acid as an intermediate, from which, after acidification with hydrogen chloride, tizanidine hydrochloride is obtained in a high yield and purity.
    Type: Grant
    Filed: December 18, 2009
    Date of Patent: July 16, 2013
    Assignee: Farmak, A.S.
    Inventors: Pavel Hradil, Lubomir Kvapil, Martin Grepl, Jan Novotny
  • Publication number: 20130177632
    Abstract: The present invention provides therapeutically effective 2,4,5-trisubstituted imidazole compounds, methods of preparing the same, and compositions comprising the compounds alone or in combination with other agents. The present invention further provides for the use of the compounds as anti-microbial agents. The anti-microbial properties of the compounds include anti-bacterial and/or anti-fungal activity.
    Type: Application
    Filed: February 27, 2013
    Publication date: July 11, 2013
    Inventors: Raed H. Al-Qawasmeh, Aiping H. Young, Mario Huesca, Yoon S. Lee
  • 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
  • Patent number: 8455529
    Abstract: The present invention relates to organic molecules capable of modulating tyrosine kinase signal transduction in order to regulate, modulate and/or inhibit abnormal cell proliferation.
    Type: Grant
    Filed: September 9, 2011
    Date of Patent: June 4, 2013
    Assignee: Allergan, Inc.
    Inventors: Julie A. Wurster, Richard C. Yee
  • Publication number: 20130137740
    Abstract: The present invention relates to specific analogs of combretastatin, in particular the compounds of formula (I) as described and defined herein, and pharmaceutical compositions comprising the compounds, as well as their medical use, in particular in the treatment or prevention of cancer, including multidrug-resistant cancer.
    Type: Application
    Filed: May 5, 2011
    Publication date: May 30, 2013
    Inventors: Rainer Schobert, Bernhard Biersack, Thomas Müller
  • Publication number: 20130131132
    Abstract: The present invention relates to N-substituted aminobenzocycloheptene, aminotetraline, aminoindane and phenalkylamine derivatives of the formula (I), (II), (III) or (IV) or a physiologically tolerated salt thereof. The invention relates to pharmaceutical compositions comprising such N-substituted aminobenzocycloheptene, aminotetraline, aminoindane and phenalkylamine derivatives, and the use of such N-substituted aminobenzocycloheptene, aminotetraline, aminoindane and phenalkylamine derivatives for therapeutic purposes. The N-substituted aminobenzocycloheptene, aminotetraline, aminoindane and phenalkylamine derivatives are GlyT1 inhibitors.
    Type: Application
    Filed: November 19, 2012
    Publication date: May 23, 2013
    Applicants: AbbVie Inc., AbbVie Deutschland GmbH & Co. KG
    Inventors: AbbVie Deutschland GmbH & Co. KG, AbbVie Inc.
  • Publication number: 20130123215
    Abstract: The present invention relates to novel 2,5-dioxoimidazolidin-1-yl-3-phenylurea derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of the N-formyl peptide receptor like-1 (FPRL-1) receptor.
    Type: Application
    Filed: November 9, 2012
    Publication date: May 16, 2013
    Applicant: ALLERGAN, INC.
    Inventor: Allergan, Inc.
  • Publication number: 20130121957
    Abstract: The present disclosure relates to compounds, compositions and methods for the treatment of Hepatitis C virus (HCV) infection. Also disclosed are pharmaceutical compositions containing such compounds and methods for using these compounds in the treatment of HCV infection.
    Type: Application
    Filed: May 7, 2012
    Publication date: May 16, 2013
    Inventors: Qi Chen, Omar D. Lopez, John A. Bender, Gan Wang, Van N. Nguyen, John F. Kadow, Nicholas A. Meanwell, Makonen Belema
  • Publication number: 20130102629
    Abstract: Compounds represented by formula (I) or pharmaceutically acceptable salts thereof, wherein A, B, B?, X, Y, R1, R2, R2?, R3, R3?, R4, R4?, R5, R5?, m, n, or p are as defined herein, are useful for treating flaviviridae viral infections.
    Type: Application
    Filed: September 24, 2012
    Publication date: April 25, 2013
    Applicant: VERTEX PHARMACEUTICALS INCORPORATED
    Inventor: Vertex Pharmaceuticals Incorporated
  • Publication number: 20130102592
    Abstract: The invention provides a compound which is an amide of the formula (1), or a salt, solvate, N-oxide or tautomer thereof; wherein: a is 0 or 1; b is 0 or 1: provided that the sum of a and b is 0 or 1; T is O or NH Ar1 is a monocyclic or bicyclic 5- to 10-membered aryl or heteroaryl group containing up to 4 heteroatoms selected from O, N and S, and being optionally substituted en by one or more substituents R1; Ar2 Js a monocyclic or bicyclic 5- to 10-membered aryl or heteroaryl group containing up to 4 heteroatoms selected from O, N and S and being optionally substituted by one or more substituents R2; and R1 and R2 are as defined in the claims. The compounds are inhibitors of kinases and in particular FLT3, FLT4 and Aurora kinases.
    Type: Application
    Filed: December 5, 2012
    Publication date: April 25, 2013
    Applicant: SAREUM LIMITED
    Inventor: Sareum Limited
  • Patent number: 8426442
    Abstract: A compound of formula (I): Or its salts or pharmaceutically acceptable derivatives thereof wherein: A represents a chemical moiety with the general formula (II): X and Y are independently selected from a group consisting of CH2, CH(R5) or C(R5)(R6); R1 is selected from the group consisting of optionally substituted arylalkyl, and optionally substituted heteroarylalkyl; R2 is selected from the group consisting of optionally substituted aryl or optionally substituted heteroaryl or NR7R8; R3 R4 R5 R6 R7 and R8 are as defined herein, n=0, 1, 2 or 3; o=0, 1 or 2, with the proviso that when o=0, then n is 1, 2 or 3 and when o=1, then n is 1 or 2 is provided. Pharmaceutical compositions comprising the compounds are also provided. These compounds are useful in the treatment of various disorders including arrhythmia.
    Type: Grant
    Filed: June 4, 2010
    Date of Patent: April 23, 2013
    Assignee: Xention Ltd
    Inventors: Richard John Hamlyn, Mushtaq Mulla, David Madge, Basil Hartzoulakis, Simon Mark Jones, Derek Edward John, Oliver Gareth Dugdale
  • Publication number: 20130081213
    Abstract: The present invention relates to a cationic 6-aminoindoline of general formula (I), the addition salts thereof with an acid and the solvates thereof: the present invention is also directed towards a method for synthesizing this cationic 6-aminoindoline, the compositions, the uses, the hair dyeing methods and the devices using this cationic 6-aminoindoline.
    Type: Application
    Filed: March 2, 2011
    Publication date: April 4, 2013
    Inventor: Aziz Fadli
  • Publication number: 20130065897
    Abstract: The present invention provides novel compounds of the Formula I, pharmaceutical compositions comprising such compounds and methods for using such compounds as agents or drugs for inhibiting perforin activity and for treating a subject at risk of or susceptible to a disease or disorder, or having a disease or disorder associated with undesirable perforin activity.
    Type: Application
    Filed: December 22, 2010
    Publication date: March 14, 2013
    Applicant: PETER MACCALLUM CANCER INSTITUTE
    Inventors: Julie Ann Spicer, Kristiina Maria Huttunen, Dani Michelle Lyons, Joseph Albert Trapani, Mark John Smyth, William Alexander Denny
  • Publication number: 20130040963
    Abstract: Described herein are compounds useful in the modulation of blood uric acid levels, formulations containing them and methods of making and using them. In some embodiments, the compounds described herein are used in the treatment or prevention of disorders related to aberrant levels of uric acid.
    Type: Application
    Filed: June 4, 2012
    Publication date: February 14, 2013
    Applicant: Ardea Biosciences, Inc.
    Inventors: Esmir GUNIC, Jean-Luc GIRARDET, David A. PAISNER
  • Publication number: 20130025618
    Abstract: The present invention relates to a cationic 4-aminoindole of general formula (I), addition salts thereof with an acid and solvates thereof: in which: R1 is a linear or branched, saturated C2-C20 alkyl radical, substituted and/or interrupted with a cationic radical. The present invention is also directed towards a process for synthesizing this cationic 4-aminoindole, to the compositions, the uses, the hair dyeing processes and the devices using this cationic 4-aminoindole.
    Type: Application
    Filed: December 6, 2010
    Publication date: January 31, 2013
    Inventor: Aziz Fadli
  • Publication number: 20130028859
    Abstract: The present disclosure relates to compounds, compositions and methods for the treatment of hepatitis C virus (HCV) infection. Also disclosed are pharmaceutical compositions containing such compounds and methods for using these compounds in the treatment of HCV infection.
    Type: Application
    Filed: January 30, 2012
    Publication date: January 31, 2013
    Inventors: John A. Bender, Omar D. Lopez, Gan Wang, Makonen Belema, John F. Kadow
  • Publication number: 20130012540
    Abstract: This disclosure concerns novel compounds of Formula (I) or as defined in the specification and compositions comprising such novel compounds. These compounds are useful antiviral agents, especially in inhibiting the function of the NS5A protein encoded by Hepatitis C virus (HCV). Thus, the disclosure also concerns a method of treating HCV related diseases or conditions by use of these novel compounds or a composition comprising such novel compounds.
    Type: Application
    Filed: September 12, 2012
    Publication date: January 10, 2013
    Inventors: Rico Lavoie, John A. Bender, Jeffrey Lee Romine, Edward H. Ruediger, Carol Bachand, Omar D. Lopez, Qi Chen, Makonen Belema, John F. Kadow, Lawrence G. Hamann
  • Publication number: 20130004457
    Abstract: The present disclosure relates to compounds, compositions and methods for the treatment of hepatitis C virus (HCV) infection. Also disclosed are pharmaceutical compositions containing such compounds and methods for using these compounds in the treatment of HCV infection.
    Type: Application
    Filed: September 11, 2012
    Publication date: January 3, 2013
    Inventors: Carol Bachand, Makonen Bekema, Daniel H. Deon, Andrew C. Good, Jason Goodrich, Clint A. James, Rico Lavoie, Omar D. Lopez, Alain Martel, Nicholas A. Meanwell, Van N. Nguyen, Jeffrey Lee Romine, Edward H. Ruediger, Lawrence B. Snyder, Denis R. St. Laurent, Fukang Yang, David R. Langley, Gan Wang, Lawrence G. Hamann
  • Publication number: 20120283298
    Abstract: Methods for administering a therapeutically effective amount of a somatostatin receptor-4 (SSTR4) agonist in order to treat learning and memory impairment for Alzheimer's disease is disclosed.
    Type: Application
    Filed: October 14, 2010
    Publication date: November 8, 2012
    Inventors: Albert Michael Crider, Kenneth A. Witt, Karin E. Sandoval
  • Publication number: 20120277217
    Abstract: Presently provided are IDO inhibitors of general formulae (VII), (VIII) as shown below and pharmaceutical compositions thereof, useful for modulating an activity of indoleamine 2,3-dioxygenase; treating indoleamine 2,3-dioxygenase (IDO) mediated immunosuppression; treating a medical conditions that benefit from the inhibition of enzymatic activity of indoleamine-2,3-dioxygenase; enhancing the effectiveness of an anti-cancer treatment comprising administering an anti-cancer agent; treating tumor-specific immunosuppression associated with cancer; and treating immunosupression associated with an infectious disease.
    Type: Application
    Filed: October 27, 2010
    Publication date: November 1, 2012
    Applicant: NewLink Genetics Corporation
    Inventors: Mario R. Mautino, Sanjeev Kumar, Firoz Jaipuri, Jesse Waldo, Tanay Kesharwani, Xiaoxia Zhang
  • Publication number: 20120277266
    Abstract: This disclosure concerns novel compounds of Formula (I) as defined in the specification and compositions comprising such novel compounds. These compounds are useful antiviral agents, especially in inhibiting the function of the NS5A protein encoded by Hepatitis C virus (HCV). Thus, the disclosure also concerns a method of treating HCV related diseases or conditions by use of these novel compounds or a composition comprising such novel compounds.
    Type: Application
    Filed: July 13, 2012
    Publication date: November 1, 2012
    Inventors: Omar D. Lopez, Qi Chen, Makonen Belema, Lawrence G. Hamann
  • Publication number: 20120252699
    Abstract: The present invention relates to novel fluorophores and their use in combination with novel nucleic acid molecules, called aptamers, that bind specifically to the fluorophore and thereby enhance the fluorescence signal of the fluorophore upon exposure to radiation of suitable wavelength. Molecular complexes formed between the novel fluorophores, novel nucleic acid molecules, and their target molecules are described, and the use of multivalent aptamer constructs as fluorescent sensors for target molecules of interest are also described.
    Type: Application
    Filed: February 18, 2010
    Publication date: October 4, 2012
    Applicant: CORNELL UNIVERSITY
    Inventors: Samie R. Jaffrey, Jeremy S. Paige
  • Publication number: 20120231972
    Abstract: The present invention relates to a probe compound that can comprise any substrate or metabolite of an enzymatic reaction in addition to an indicator component, such as, for example, a fluorescence dye, or the like. Moreover, the present invention relates to means for detecting enzymes in form of an array, which comprises any number of probe compounds of the invention which each comprise a different metabolite of interconnected metabolites representing the central pathways in all forms of life. Moreover, the present invention relates to a method for detecting enzymes involving the application of cell extracts or the like to the array of the invention which leads to reproducible enzymatic reactions with the substrates. These specific enzymatic reactions trigger the indicator (e.g. a fluorescence signal) and bind the enzymes to the respective cognate substrates. Moreover, the invention relates to means for isolating enzymes in form of nanoparticles coated with the probe compound of the invention.
    Type: Application
    Filed: March 19, 2010
    Publication date: September 13, 2012
    Inventors: Peter N. Golyshin, Olga V. Golyshina, Kenneth N. Timmis, Tatyana Chernikova, Agnes Waliczek, Manuel Ferrer, Ana Beloqul, Maria E. Guazzaroni, Jose M. Vieltes, Florencio Pazos, Antonio Lopez De Lacey, Victor M. Fernandez
  • Publication number: 20120220622
    Abstract: The present invention relates to a heterocyclic derivative of formula (I) wherein the variables are as defined in the specification, or to a pharmaceutically acceptable salt or solvate thereof. The present invention further relates to pharmaceutical compositions comprising said heterocyclic derivatives and to their use in therapy, for instance in the treatment or prevention of disorders mediated by glutamate dysfunction, such as schizophrenia and generalised anxiety disorder.
    Type: Application
    Filed: November 2, 2010
    Publication date: August 30, 2012
    Inventors: Julia Adam, Jonathan Gillespie, Steven Laats, John Kinnaird Ferguson MacLean, Duncan Robert McArthur
  • Patent number: 8252923
    Abstract: The present invention relates to peptidomimetic compounds useful as protease inhibitors, particularly as serine protease inhibitors and more particularly as hepatitis C NS3 protease inhibitors; intermediates thereto; their preparation including novel steroselective processes to intermediates. The invention is also directed to pharmaceutical compositions and to methods for using the compounds for inhibiting HCV protease or treating a patient suffering from an HCV infection or physiological condition related to the infection. Also provided are pharmaceutical combinations comprising, in addition to one or more HCV serine protease inhibitors, one or more interferons exhibiting anti-HCV activity and/or one or more compounds having anti HCV activity and a pharmaceutically acceptable carrier, and methods for treating or preventing a HCV infection in a patient using the compositions. The present invention is also directed to a kit or pharmaceutical pack for treating or preventing HCV infection in a patient.
    Type: Grant
    Filed: September 8, 2008
    Date of Patent: August 28, 2012
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: Robert Edward Babine, Shu-Hui Chen, Jason Eric Lamar, Nancy June Snyder, Xicheng Sun, Mark Joseph Tebbe, Frantz Victor, Q. May Wang, Yvonne Yee Mai Yip, Ivan Collado, Cristina Garcia-Paredes, Raymond Samuel Parker, III, Ling Jin, Deqi Guo, John Irvin Glass
  • Publication number: 20120195857
    Abstract: The present disclosure relates to compounds, compositions and methods for the treatment of hepatitis C virus (HCV) infection. Also disclosed are pharmaceutical compositions containing such compounds and methods for using these compounds in the treatment of HCV infection.
    Type: Application
    Filed: August 4, 2011
    Publication date: August 2, 2012
    Inventors: Makonen Belema, Pothukanuri Srinivasu, John A. Bender, Omar D. Lopez, Qi Chen, Richard A. Rampulla, Samayamunthula Venkata Satya Arun Kumar Gupta, Nicholas A. Meanwell
  • Patent number: 8232312
    Abstract: The present invention relates to substituted arylsulphonylglycines of general formula (I) wherein R, X, Y and Z are defined as in claim 1, the tautomers, enantiomers, diastereomers, mixtures thereof and salts thereof, which have valuable pharmacological properties, particularly the suppression of the interaction of glycogen phosphorylase a with the GL subunit of glycogen-associated protein phosphatase 1 (PP1), and their use as pharmaceutical compositions.
    Type: Grant
    Filed: March 14, 2008
    Date of Patent: July 31, 2012
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Holger Wagner, Elke Langkopf, Matthias Eckhardt, Ruediger Streicher, Corinna Schoelch, Annette Schuler-Metz, Alexander Pautsch
  • Publication number: 20120190680
    Abstract: Compounds, pharmaceutical compositions, and methods of use are disclosed for heteroaryl amide analogues of formula Ia and/or Ib: In certain embodiments, the heteroaryl amide analogues are agonists and/or ligands of dopamine receptors and may be useful, inter alia, for the treatment of a condition responsive to P2X7 receptor modulation, for example, pain, inflammation, a neurological or neurodegenerative disorder, a cardiovascular disorder, an ocular disorder or an immune system disorder.
    Type: Application
    Filed: August 11, 2008
    Publication date: July 26, 2012
    Applicant: H. LUNDBECK A/S
    Inventors: Rajagopal Bakthavatchalam, David C. Ihle, Scott M. Capitosti, David J. Wustrow, Jun Yuan
  • Publication number: 20120184582
    Abstract: The present invention relates to novel compounds which are effective as an inhibitor for xanthine oxidase, a process for preparing the same, and a pharmaceutical composition comprising a therapeutically effective amount of the same.
    Type: Application
    Filed: October 4, 2010
    Publication date: July 19, 2012
    Inventors: Jeong Uk Song, Geun Tae Kim, Sung Pil Choi, Cheol Kyu Jung, Deok Seong Park, Eun Sil Choi, Tae Hun Kim, Hyun Jung Park, Wan Su Park, Heui Sul Park, Ki Chul Koo, Vasily Artemov
  • Publication number: 20120178764
    Abstract: The present invention relates to substituted indoles useful as pharmaceutical compounds for treating respiratory disorders.
    Type: Application
    Filed: January 5, 2012
    Publication date: July 12, 2012
    Inventors: Roger Bonnert, Rukhsana (née RASUL, Rukhsana) Mohammed, Mark Robert Dickinson
  • Publication number: 20120149702
    Abstract: The present invention relates to compounds and pharmaceutical preparations and their use in therapy for preventing or treating trauma, ischemia, stroke and degenerative diseases associated with cell death. Methods and compositions of the invention are particularly useful for treating neurological disorders associated with cellular necrosis.
    Type: Application
    Filed: February 21, 2012
    Publication date: June 14, 2012
    Applicants: The Brigham and Women's Hospital, Inc., President and Fellows of Harvard College
    Inventors: Gregory D. Cuny, Prakash Jagtap, Junying Yuan, Alexei Degterev
  • Publication number: 20120135997
    Abstract: The present invention provides, for example, the following compounds as a pharmaceutical composition for treating diseases induced by production, secretion or deposition of amyloid ? proteins. The present invention provides a pharmaceutical composition for suppressing amyloid ? production comprising a compound of the formula: wherein A is a benzene ring, a pyridine ring or a pyrimidine ring, X is sultam, lactam, sulfonamide or the like, C is substituted or unsubstituted imidazolyl, substituted or unsubstituted oxazolyl or the like, R2, R3 and R4 are each independently hydrogen, halogen, hydroxy, carboxy, substituted or unsubstituted alkyl, substituted or unsubstituted alkoxy or the like, its pharmaceutically acceptable salt or a solvate thereof.
    Type: Application
    Filed: July 15, 2010
    Publication date: May 31, 2012
    Applicant: Shionogi & Co., Ltd.
    Inventors: Issei Kato, Kazuya Kano
  • Publication number: 20120122854
    Abstract: The invention is concerned with novel carbocyclyl fused cyclic amines of formula (I) wherein A, X1 to X3, Y1 to Y3, Z, R1, R2, m and n are as defined in the description and in the claims, as well as physiologically acceptable salts thereof. These compounds inhibit the coagulation factor Xa and can be used as medicaments.
    Type: Application
    Filed: January 11, 2012
    Publication date: May 17, 2012
    Inventors: Markus Boehringer, Katrin Groebke Zbinden, Wolfgang Haap, Narendra Panday, Fabienne Ricklin, Martin Stahl, Petra Schmitz
  • Patent number: 8178687
    Abstract: Pyrroloindoles of formula (I) are provided wherein Het is an aromatic or partially unsaturated, monocyclic or bicyclic heterocycle containing between 1 and 4 heteroatoms N, O or S, optionally substituted by R1 or R?1 which are the same or different; R is X-(A-B)n-CONH2, X-(A-B)n-O—CONH2, X-(A-B)n-NH—CONH2, X—(CH2)m-heterocycloalkyl, X(CH2)m-aryl and X—(CH2)m-heteroaryl wherein X is —O—C(O), —NH—C(O), NH—CS, —NH—CO—CH2-O—; —NH—COCH2-S—CH2-CO—NH—; —NH—CO—(CH2)2-SO2-; and —NH—CO—CH2-N(CH3)-CO—; A and B are the same or different and are each independently a single bond, CH2, CH-alkyl, and CH-aralkyl; n=1, 2 and m=0, 1; R1 and/or R?1 are H, halogen, CF3, nitro, cyano, alkyle, hydroxy, mercapto, amino, alkylamino, dialkylamino, alkoxy, alkylthio, and carboxy, free or esterified by an alkyl, carboxamide, CONH(alkyl), CON(alkyl)2, NH—CO-alkyl, sulfonamide, NH—SO2-alkyl, S(O)2-NHalkyl, and S(O2)-N(alkyl)2 group, all of said alkyl, alcoxy and alkylthio groups being optionally substituted themselves, said products being
    Type: Grant
    Filed: December 16, 2010
    Date of Patent: May 15, 2012
    Assignee: Sanofi-Aventis
    Inventors: Marcel Alasia, Hervé Minoux, Jean-Marie Ruxer
  • Patent number: 8178553
    Abstract: This invention relates to compounds of the Formula (I): or a pharmaceutically acceptable salt, solvate or isomer thereof, which can be useful for the treatment of diseases or conditions mediated by MMPs, ADAMs, TACE, aggrecanase, TNF-? or combinations thereof.
    Type: Grant
    Filed: January 20, 2010
    Date of Patent: May 15, 2012
    Assignee: Schering Corporation
    Inventors: Brian J. Lavey, Joseph A. Kozlowski, Guowei Zhou, Ling Tong, Wensheng Yu, Michael K. C. Wong, Shankar B. Bandarpalle, Neng-Yang Shih, M. Arshad Siddiqui, Kristin E. Rosner, Chaoyang Dai, Janeta Popovici-Muller, Vinay M. Girijavallabhan, Dansu Li, Aneta Maria Kosinski, Seong-Heon Kim, De-Yi Yang, Razia K. Rizvi
  • Publication number: 20120077811
    Abstract: The invention provides novel prodrug compounds comprising a kinase inhibitor and a reductively-activated fragmenting aromatic nitroheterocycle or aromatic nitrocarbocycle trigger, where the compound carries a positive charge. In preferred embodiments, the compounds are of Formula I: where: X is any negatively charged counterion; R1 is a group of the formula —(CH2)nTr, where Tr is an aromatic nitroheterocycle or aromatic nitrocarbocycle and —(CH2)nTr acts as a reductively-activated fragmenting trigger; and n is an integer from 0 to 6; R2, R3 and R4 may each independently be selected from aliphatic or aromatic groups of a tertiary amine kinase inhibitor (R2)(R3)(R4)N, or two of R2, R3, and R4 may form an aliphatic or aromatic heterocyclic amine ring of a kinase inhibitor, or one of R2, R3 and R4 may be absent and two of R2, R3 and R4 form an aromatic heterocyclic amine ring of a kinase inhibitor. The compounds of the invention are useful in treating proliferative diseases such as cancer.
    Type: Application
    Filed: March 11, 2010
    Publication date: March 29, 2012
    Inventors: Jeffrey Bruce Smaill, Adam Vorn Patterson, Michael Patrick Hay, William Alexander Denny, William Robert Wilson, Guo-Liang Lu, Robert Forbes Anderson, Ho Huat Lee, Amir Ashoorzadeh
  • Publication number: 20120071524
    Abstract: The present invention relates to novel compounds having anti-cancer activity, methods of making these compounds, and their use for treating cancer and drug-resistant tumors, e.g. melanoma, metastatic melanoma, drug resistant melanoma, prostate cancer and drug resistant prostate cancer.
    Type: Application
    Filed: August 24, 2011
    Publication date: March 22, 2012
    Inventors: Yan Lu, Chien-Ming Li, Zhao Wang, Jianjun Chen, Wei Li, James T. DALTON, Duane D. Miller, Charles Duke, Sunjoo Ahn
  • Publication number: 20120053165
    Abstract: Compounds and pharmaceutically acceptable salts of the compounds are disclosed, wherein the compounds have the structure of Formula (I) as defined in the specification. Corresponding pharmaceutical compositions, methods of treatment, methods of synthesis, and intermediates are also disclosed.
    Type: Application
    Filed: March 2, 2010
    Publication date: March 1, 2012
    Applicant: Pfizer Inc.
    Inventors: Martin Patrick Allen, Christopher William Am Ende, Michael Aaron Brodney, Amy Beth Dounay, Douglas Scott Johnson, Martin Youngjin Pettersson, Jacob Bradley Schwartz, Tuan Phong Tran
  • Publication number: 20120022057
    Abstract: The present invention relates to novel heterocyclic compounds as diacylglycerol acyltransferase (“DGAT”) inhibitors, pharmaceutical compositions comprising the heterocyclic compounds and the use of the compounds for treating or preventing a cardiovascular disease, a metabolic disorder, obesity or an obesity-related disorder, diabetes, dyslipidemia, a diabetic complication, impaired glucose tolerance or impaired fasting glucose. An illustrative compound of the invention is shown below (I).
    Type: Application
    Filed: March 16, 2010
    Publication date: January 26, 2012
    Applicant: Schering Corporation
    Inventors: Gang Zhou, Grant Wishart, Pauline C. Ting, Robert G. Aslanian, Nicolas Zorn, Jianhua Cao
  • Patent number: 8101608
    Abstract: The invention provides a novel class of compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with abnormal or deregulated kinase activity, particularly diseases or disorders that involve abnormal activation of the Abl, Bcr-Abl, cSrc, TPR-Met, Tie2, MET, FGFR3, Aurora, Axl, Bmx, BTK, c-kit, CHK2, Flt3, MST2, p70S6K, PDGFR, PKB, PKC, Raf, ROCK-II, Rsk1, SGK, TrkA, TrkB and TrkC kinases.
    Type: Grant
    Filed: November 7, 2005
    Date of Patent: January 24, 2012
    Assignee: IRM LLC, a Delware Limited Corporation
    Inventors: Yongqin Wan, Yuan Mi, Yi Fan, Dai Cheng, Yi Liu, Nathanael S. Gray, Pamela Albaugh