Three Or More Ring Hetero Atoms In The Tetracyclo Ring System Patents (Class 544/247)
  • Patent number: 10106540
    Abstract: The present invention relates to small molecule compounds and their use as HDAC inhibitors and in the treatment of various diseases, such as cancer. The present invention further relates to methods of synthesizing the compounds and methods of treatment. H-L(HA), H is a head group selected from (head group 1), (head group 2), (head group 3), (head group 4), (head group 5) and (head group 6).
    Type: Grant
    Filed: August 4, 2015
    Date of Patent: October 23, 2018
    Assignees: UNIVERSITÄT REGENSBURG, FRIEDRICH-SCHILLER-UNIVERSITÄT JENA, UNIVERSITÄTSKLINIKUM JENA
    Inventors: Siavosh Mahboobi, Andreas Sellmer, Herwig Pongratz, Michel Leonhardt, Oliver Krämer, Frank-Dietmar Böhmer, Gerhard Kelter
  • Patent number: 9469647
    Abstract: The present invention relates to acid addition salt and salt crystals of (6aR,9aS)-5,6a,7,8,9,9a-hexahydro-5-methyl-3-(phenylamino)-2-((4-(6-fluoropyridin-2-yl)phenyl)methyl)-cyclopent[4,5]imidazo[1,2-a]pyrazolo[4,3-e]pyrimidin-4(2H)-one, composition comprising the same and the method of making and using such salt and crystal.
    Type: Grant
    Filed: June 21, 2013
    Date of Patent: October 18, 2016
    Assignee: INTRA-CELLULAR THERAPIES, INC.
    Inventors: Peng Li, Lawrence P. Wennogle, Robert Davis, Graham Buckton, Mark Hooper
  • Patent number: 9040519
    Abstract: This disclosure is directed to fused tetracyclic pyrido[4,3-b>]indole and pyrido[3,4-b]indole derivatives. Pharmaceutical compositions comprising the compounds are also provided, as are methods of using the compounds in a variety of therapeutic applications, including the treatment of a cognitive disorder, psychotic disorder, neurotransmitter-mediated disorder and/or a neuronal disorder.
    Type: Grant
    Filed: February 18, 2011
    Date of Patent: May 26, 2015
    Assignee: Medivation Technologies, Inc.
    Inventors: Sarvajit Chakravarty, Barry Patrick Hart, Rajendra Parasmal Jain
  • Publication number: 20150141410
    Abstract: Chemical compounds are provided which act on GPR17 receptors and are useful in the treatment or amelioration of chronic and/or acute neurodegenerative diseases, such as multiple sclerosis, inflammatory diseases, pathologies involving the immune system, cardiovascular diseases, and renal diseases.
    Type: Application
    Filed: May 9, 2012
    Publication date: May 21, 2015
    Applicants: UNIVERSITA' DEGLI STUDI DI MILANO, FONDAZIONE ITALIANA SCLEROSI MULTIPLA - FISH ONLUS
    Inventors: Maria Pia Abbracchio, Mario Alberto Battaglia, Ivano Eberini, Marta Fumagalli, Chiara Parravicini, Cristina Sensi, Paola Zaratin
  • Publication number: 20150139915
    Abstract: Methods and compositions are described for reducing airway reactivity and the susceptibility to asthmatic bronchoconstriction that involve increasing sphingolipid content in airways and lungs of a mammalian subject.
    Type: Application
    Filed: May 16, 2013
    Publication date: May 21, 2015
    Inventors: Stefan Worgall, Tilla S. Worgall
  • Patent number: 9034655
    Abstract: Luminescent labels based on aromatic and heterocyclic compounds, including reactive intermediates used to synthesize these compounds, and methods of synthesizing and using these reporter compounds. These labels combine high photostabilities, large Stokes' shifts and contain a pyrimidinium moiety as a water-soluble group. These luminescent compounds relate generally to the following structure: The methods relate generally to the synthesis and/or use of reporter compounds for fluorescence lifetime or fluorescence polarization based applications.
    Type: Grant
    Filed: October 18, 2010
    Date of Patent: May 19, 2015
    Assignee: SETA BioMedicals, LLC
    Inventors: Leonid D. Patsenker, Inna G. Yermolenko, Iryna A. Fedyunyaeva, Yelena N. Obukhova, Olga N. Semenova, Ewald A. Terpetschnig
  • Publication number: 20150126502
    Abstract: The present invention provides compounds having a structure according to Formula (I): or a salt or solvate thereof, wherein ring A, X, R1, R2, R3, R4, R5 and R6, are defined herein. The invention further provides pharmaceutical compositions including the compounds of the invention and methods of making and using the compounds and compositions of the invention, e.g., in the treatment and prevention of various disorders, such as Parkinson's disease.
    Type: Application
    Filed: January 14, 2015
    Publication date: May 7, 2015
    Inventors: Robert A. GALEMMO, Dean R. ARTIS, Xiaocong Michael YE, Danielle Aubele, Anh TRUONG, Simeon BOWERS, Roy K. Hom, Yong-Liang ZHU, R. Jeffrey NEITZ, Jennifer SEALY, Marc ADLER, Paul BEROZA, John P. ANDERSON
  • Patent number: 9006258
    Abstract: The present invention relates to a new use for compounds that inhibit phosphodiesterase 1 (PDE1), e.g., that inhibit PDE1-mediated suppression of the dopamine D1 receptor and/or progesterone signaling pathways, including, e.g., methods of treatment or prophylaxis for conditions which may be ameliorated by enhancing the progesterone signaling response, particularly female sexual dysfunction.
    Type: Grant
    Filed: December 5, 2007
    Date of Patent: April 14, 2015
    Assignee: Intra-Cellular Therapies, Inc.
    Inventors: Allen A. Fienberg, Sharon Mates, Lawrence P. Wennogle
  • Publication number: 20150080357
    Abstract: Optionally substituted 4,5,7,8-tetrahydro-(optionally 4-thioxo or 4-imino)-(1H or 2H)-imidazo[1,2-a]pyrazolo[4,3-e]pyrimidine or 4,5,7,8,9-pentahydro-(optionally 4-thioxo or 4-imino)-(1H or 2H)-pyrimido[1,2-a]pyrazolo[4,3-e]pyrimidine compounds or Compounds of Formula (I), processes for their production, their use as pharmaceuticals and pharmaceutical compositions comprising them.
    Type: Application
    Filed: June 4, 2014
    Publication date: March 19, 2015
    Inventors: Peng LI, Jun ZHAO, Hailin ZHENG, Lawrence WENNOGLE
  • Publication number: 20150072965
    Abstract: Optionally substituted 4,5,7,8-tetrahydro-(optionally 4-oxo, 4-thioxo or 4-imino)-2H-imidazo[1,2-a]pyrrolo[3,4-e]pyrimidine or 4,5,7,8,9-pentahydro-(optionally 4-oxo, 4-thioxo or 4-imino)-2H-pyrimido[1,2-a]pyrrolo[3,4-e]pyrimidine compounds or Compounds of Formula (I), processes for their production, their use as pharmaceuticals and pharmaceutical compositions comprising the same.
    Type: Application
    Filed: November 12, 2014
    Publication date: March 12, 2015
    Inventors: Peng LI, Jun ZHAO, Hailin ZHENG, Lawrence WENNOGLE
  • Publication number: 20150062694
    Abstract: The present invention is related to 6,7-dihydrobenzimidazo[1,2-c]quinazolin-6-one derivatives of the general structural formula (I), the anisotropic optical film based on these derivatives with phase-retarding properties for displays, and method of producing thereof: where X is a carboxylic group COOH, m is 0, 1, 2 or 3; Y is a sulfonic group SO3H, n is 0, 1, 2 or 3; Z is an acid amide group L-NH2; p is 0, 1, 2 or 3; K is a counterion selected from the list comprising H+, NH4+, Na+, K+, Li+, Mg2+, Ca2+, Zn2+, and Al3+; s is the number of counterions providing neutral state of the molecule; R is a substituent selected from the list comprising CH3, C2H5, NO2, Cl, Br, F, CF3, CN, OH, OCH3, OC2H5, OCOCH3, OCN, SCN, NH2, and NHCOCH3; w is 0, 1, 2, 3 or 4; and R1 is a substituent selected from the list comprising H, CH3, C2H5, C3H7, i-C3H7, CH2CH2CH2CH3, CH(CH3)CH2CH3, CH2CH(CH3)CH3 and C(CH3)3 and L is a linking group.
    Type: Application
    Filed: September 16, 2014
    Publication date: March 5, 2015
    Applicant: CRYSOPTIX KK
    Inventors: Tatyana Doutova, Pavel I. Lazarev, Elena N. Sidorenko
  • Publication number: 20150038474
    Abstract: Optionally substituted 3-(thio, sulfinyl or sulfonyl)-7,8-dihydro-(1H or 2H)-imidazo[1,2-a]pyrazolo[4,3-e]pyrimidin-4(5H)-one or a substituted 3-(thio, sulfinyl or sulfonyl)-7,8,9-trihydro-(1H or 2H)-pyrimido[1,2-a]pyrazolo[4,3-e]pyrimidin-4(5H)-one compounds or Compounds of Formula (I), processes for their production, their use as pharmaceuticals and pharmaceutical compositions comprising them.
    Type: Application
    Filed: October 3, 2014
    Publication date: February 5, 2015
    Inventors: Peng LI, Jun ZHAO, Hailin ZHENG, Lawrence P. WENNOGLE
  • Patent number: 8937150
    Abstract: Compounds effective in inhibiting replication of Hepatitis C virus (“HCV”) are described. This invention also relates to processes of making such compounds, compositions comprising such compounds, and methods of using such compounds to treat HCV infection.
    Type: Grant
    Filed: May 4, 2011
    Date of Patent: January 20, 2015
    Assignee: AbbVie Inc.
    Inventors: David A. DeGoey, Warren M. Kati, Charles W. Hutchins, Pamela L. Donner, Allan C. Krueger, John T. Randolph, Christopher E. Motter, Lissa T. Nelson, Sachin V. Patel, Mark A. Matulenko, Ryan G. Keddy, Tammie K. Jinkerson, Yi Gao, Dachun Liu, John K. Pratt, Todd W. Rockway, Clarence J. Maring, Douglas K. Hutchinson, Charles A. Flentge, Rolf Wagner, Michael D. Tufano, David A. Betebenner, Kathy Sarris, Kevin R. Woller, Seble H. Wagaw, Jean C. Califano, Wenke Li, Daniel D. Caspi, Mary E. Bellizzi, William A. Carroll
  • Patent number: 8921514
    Abstract: Compounds effective in inhibiting replication of Hepatitis C virus (“HCV”) are described. This invention also relates to processes of making such compounds, compositions comprising such compounds, and methods of using such compounds to treat HCV infection.
    Type: Grant
    Filed: December 9, 2010
    Date of Patent: December 30, 2014
    Assignee: AbbVie Inc.
    Inventors: David A. DeGoey, Warren M. Kati, Charles W. Hutchins, Pamela L. Donner, Allan C. Krueger, John T. Randolph, Christopher E. Motter, Lissa T. Nelson, Sachin V. Patel, Mark A. Matulenko, Ryan G. Keddy, Tammie K. Jinkerson, Yi Gao, Dachun Liu, John K. Pratt, Todd W. Rockway, Clarence J. Maring, Douglas K. Hutchinson, Charles A. Flentge, Rolf Wagner, Michael D. Tufano, David A. Betebenner, Kathy Sarris, Kevin R. Woller, Seble H. Wagaw, Jean C. Califano, Wenke Li, Daniel D. Caspi, Mary E. Bellizzi, William A. Carroll
  • Patent number: 8920944
    Abstract: Use of a precursor of an n-dopant for doping an organic semiconductive material, as a blocking layer, as a charge injection layer, as an electrode material, as a storage material or as a semiconductor material itself in electronic or optoelectronic components, the precursor being selected from the following formulae 1-3c:
    Type: Grant
    Filed: June 20, 2008
    Date of Patent: December 30, 2014
    Assignee: Novaled AG
    Inventors: Michael Limmert, Andrea Lux, Horst Hartmann
  • Publication number: 20140357606
    Abstract: 1- or 2-substituted (6aR,9aS)-3-(phenylamino)-5-6a,7,8,9,9a-hexahydro-5-methyl-cyclopent[4,5]imidazo[1,2-a]pyrazolo[4,3-e]pyrimidin-4(1H or, 2H)-one compounds of Formula (I), processes for their production, their use as pharmaceuticals and pharmaceutical compositions comprising them.
    Type: Application
    Filed: August 15, 2014
    Publication date: December 4, 2014
    Inventor: Peng LI
  • Patent number: 8901300
    Abstract: Provided are tetraazapyrene compounds of formula (I) and their use as n-type semiconductors. In formula (I), R1, R2, R3, R4, at each occurrence, independently are selected from H, a C1-30 alkyl group, a C1-30 alkoxy group, a C1-30 alkylthio group, a C6-14 aryl group, a C6-14 aryloxy group, a C6-14 arylthio group, a C7-20 arylalkyl group, CI and Br; R5, R6, at each occurrence, independently are selected from H, a C1-30 alkyl group, a Cy1-30 haloalkyl group, a C6-14 aryl group and a C7-20 arylalkyl group, wherein aryl and arylalkyl can be optionally substituted with one or more halogen, C1-4 haloalkyl, —CN, —NO2, —CHO, —COOH, —CONH2, —CO(C1-14 alkyl), —COO(C1-14 alkyl), CONHC(C1-14 alkyl) and —CON(C1-14 alkyl)2 groups, with the proviso that at least one of R1, R2, R3, R4 is a C6-14 aryloxy, a C6-14 arylthio I group, CI or Br. (I).
    Type: Grant
    Filed: February 16, 2012
    Date of Patent: December 2, 2014
    Assignee: BASF SE
    Inventors: Nicolle Langer, Sonja Geib, Susanne Martens, Lutz Gade
  • Publication number: 20140323717
    Abstract: Special C-functionalized cyclic bisaminal compounds having formula (I) or (II), their salts or solvates, methods for their preparation, their uses, and methods for preparing functional tetraazacycloalkane compounds implementing such cyclic bisaminal compounds.
    Type: Application
    Filed: November 16, 2012
    Publication date: October 30, 2014
    Inventors: Raphael Tripier, Nathalie Camus
  • Patent number: 8865895
    Abstract: The present invention is related to 6,7-dihydrobenzimidazo[1,2-c]quinazolin-6-one derivatives of the general structural formula (I), where X is a carboxylic group COOH, m is 0, 1, 2 or 3; Y is a sulfonic group SO3H, n is 0, 1, 2 or 3; Z is an acid amide group L-NH2; p is 0, 1, 2 or 3; K is a counterion selected from the list comprising H+, NH4+, Na+, K+, Li+, Mg2+, Ca2+, Zn2+, and Al3+; s is the number of counterions providing neutral state of the molecule; R is a substituent selected from the list comprising CH3, C2H5, NO2, Cl, Br, F, CF3, CN, OH, OCH3, OC2H5, OCOCH3, OCN, SCN, NH2, and NHCOCH3; w is 0, 1, 2, 3 or 4; and R1 is a substituent selected from the list comprising H, CH3, C2H5, C3H7, i-C3H7, CH2CH2CH2CH3, CH(CH3)CH2CH3, CH2CH(CH3)CH3 and C(CH3)3 and L is a linking group.
    Type: Grant
    Filed: January 15, 2007
    Date of Patent: October 21, 2014
    Assignee: Crysoptix K.K.
    Inventors: Tatyana Doutova, Pavel I. Lazarev, Elena N. Sidorenko
  • Publication number: 20140303144
    Abstract: Hydrogenated pyrido[4,3-b]indoles, pyrido[3,4-b]indoles and azepino[4,5-b]indoles are described. The compounds may bind to and are adrenergic receptor ?2B antagonists. The compounds may also bind to and antagonize adrenergic receptor ?2B. The compounds may find use in therapy, e.g., to (i) reduce blood pressure and/or (ii) promote renal blood flow and/or (iii) decrease or inhibit sodium reabsorption. The compounds may also be used to treat diseases or conditions that are, or are expected to be, responsive to a decrease in blood pressure. Use of the compounds to treat cardiovascular and renal disorders is particularly described.
    Type: Application
    Filed: February 17, 2012
    Publication date: October 9, 2014
    Applicant: Medivation Technologies, Inc.
    Inventors: Andrew Asher Protter, Sarvajit Chakravarty
  • Patent number: 8829008
    Abstract: 1- or 2-substituted (6aR,9aS)-3-(phenylamino)-5-6a,7,8,9,9a-hexahydro-5-methyl-cyclopent[4,5]imidazo[1,2-a]pyrazolo[4,3-e]pyrimidin-4(1H or, 2H)-one compounds of Formula (I), processes for their production, their use as pharmaceuticals and pharmaceutical compositions comprising them.
    Type: Grant
    Filed: June 1, 2012
    Date of Patent: September 9, 2014
    Assignee: Takeda Pharmaceutical Company Limited
    Inventor: Peng Li
  • Publication number: 20140228353
    Abstract: Hydrogenated pyrido[4,3-b]indoles, pyrido[3,4-b]indoles and azepino[4,5-b]indoles are described. The compounds may bind to and are antagonists of the adrenergic receptor ?2A. The compounds may also bind to and are an antagonist of the adrenergic receptor ?2B; or the compounds are not antagonists of the adrenergic receptor ?2B and the compounds are administered in conjunction with a second agent that reduces, or is expected to reduce, blood pressure in an individual. The compounds may find use in therapy, e.g., to regulate blood glucose level, increase insulin secretion and treat diseases or conditions that are, or are expected to be, responsive to an increase in insulin production. Use of the compounds to treat type 2 diabetes is particularly described.
    Type: Application
    Filed: February 17, 2012
    Publication date: August 14, 2014
    Applicant: Medivation Technologies, Inc.
    Inventors: Andrew Asher Protter, Sarvvajit Chakravarty
  • Publication number: 20140221356
    Abstract: Compounds for use in the treatment of human immunodeficiency virus (HIV) infection are disclosed. The compounds have the following Formula (I): including stereoisomers and pharmaceutically acceptable salts thereof, wherein R1, X, W, Y1, Y2, Z1, and Z4 are as defined herein. Methods associated with preparation and use of such compounds, as well as pharmaceutical compositions comprising such compounds, are also disclosed.
    Type: Application
    Filed: December 19, 2013
    Publication date: August 7, 2014
    Inventors: Haolun JIN, Scott E. LAZERWITH, Teresa Alejandra TREJO MARTIN, Elizabeth M. BACON, Jeromy J. COTTELL, Zhenhong R. CAI, Hyung-Jung PYUN, Philip Anthony MORGANELLI, Mingzhe JI, James G. TAYLOR, Xiaowu CHEN, Michael R. MISH, Manoj C. DESAI
  • Publication number: 20140221355
    Abstract: Compounds for use in the treatment of human immunodeficiency virus (HIV) infection are disclosed. The compounds have the following Formula (I): including stereoisomers and pharmaceutically acceptable salts thereof, wherein R1, X, W, Y1, Y2, Z1, Z2, or Z4 are as defined herein. Methods associated with preparation and use of such compounds, as well as pharmaceutical compositions comprising such compounds, are also disclosed.
    Type: Application
    Filed: December 19, 2013
    Publication date: August 7, 2014
    Inventors: Scott E. LAZERWITH, Haolun JIN, Hyung-Jung Pyun
  • Publication number: 20140194396
    Abstract: The present invention relates to PDEI inhibitory compounds of Formula I as described herein, processes for their production, their use as pharmaceuticals and pharmaceutical compositions comprising them.
    Type: Application
    Filed: June 11, 2012
    Publication date: July 10, 2014
    Applicant: INTRA-CELLULAR THERAPIES, INC.
    Inventors: Peng Li, Hlilin Zheng, Jun Zhao, Lawrence P. Wennogle
  • Patent number: 8772301
    Abstract: Provided herein are compounds and methods of synthesis thereof. The compounds set forth herein are useful for the treatment, prevention, and/or management of various disorders, such as neurological disorders, neurodegenerative disorders, neuropsychiatric disorders, disorders of cognition, learning or memory, gastrointestinal disorders, lower urinary tract disorder, and cancer. Compounds set forth herein modulate the activity of metabotropic glutamate receptor 5 (mGluR5) in the central nervous system or the periphery. Pharmaceutical formulations containing the compounds and their methods of use are also provided herein.
    Type: Grant
    Filed: December 17, 2010
    Date of Patent: July 8, 2014
    Assignee: Sunovion Pharmaceuticals, Inc.
    Inventors: Larry Wendell Hardy, Michele L. R. Heffernan, Frank Xinhe Wu, Kerry L. Spear, Lakshmi D. Saraswat
  • Publication number: 20140148421
    Abstract: Optionally substituted 4,5,7,8-tetrahydro-(optionally 4-oxo, 4-thioxo or 4-imino)-2H-imidazo[1,2-a]pyrrolo[3,4-e]pyrimidine or 4,5,7,8,9-pentahydro-(optionally 4-oxo, 4-thioxo or 4-imino)-2H-pyrimido[1,2-a]pyrrolo[3,4-e]pyrimidine compounds or Compounds of Formula (I), processes for their production, their use as pharmaceuticals and pharmaceutical compositions comprising the same.
    Type: Application
    Filed: January 31, 2014
    Publication date: May 29, 2014
    Applicant: INTRA-CELLULAR THERAPIES, INC.
    Inventors: Peng LI, Jun ZHAO, Hailin ZHENG, Lawrence WENNOGLE
  • Publication number: 20140080821
    Abstract: Provided herein are benzopyrimido-pyrrolo-oxazine-dione (BPO) compounds and pyrimido-pyrrolo-quinoxalinedione (PPQ) compounds, and compositions comprising these compounds, that inhibit cystic fibrosis transmembrane conductance regulator (CFTR) mediated ion transport and that are useful for treating diseases and disorders associated with aberrantly increased CFTR chloride channel activity, such as polycystic kidney disease and secretory diarrheas. The compounds and compositions comprising the compounds described herein may be used for inhibiting expansion or preventing formation of cysts in persons who have polycystic kidney disease.
    Type: Application
    Filed: May 25, 2012
    Publication date: March 20, 2014
    Applicant: The Regents of the University of California
    Inventors: Alan S. Verkman, David S. Snyder
  • Patent number: 8637666
    Abstract: A method of preparing a compound represented by Structural Formula (I): or a pharmaceutically acceptable salt thereof, wherein the variables of Structural Formula (I) are as described in the specification and claims, comprises the step of: a) cyclizing a compound represented by Structural Formula A: under suitable reductive cyclization conditions to form a compound represented by Structural Formula B: wherein R10 is LG1 or —X1R1, and -LG1 is a suitable leaving group; and b) optionally, when R10 of Structural Formula (B) is LG1, further comprising the step of replacing the -LG1 of Structural Formula (B) with —X1R1 to form the compound represented by Structural Formula (I).
    Type: Grant
    Filed: March 20, 2012
    Date of Patent: January 28, 2014
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: Jean-Damien Charrier, Steven Durrant, David Kay
  • Patent number: 8633180
    Abstract: Optionally substituted 4,5,7,8-tetrahydro-(optionally 4-thioxo or 4-imino)-(1H or 2H)-imidazo[1,2-a]pyrazolo[4,3-e]pyrimidine or 4,5,7,8,9-pentahydro-(optionally 4-thioxo or 4-imino)-(1H or 2H)-pyrimido[1,2-a]pyrazolo[4,3-e]pyrimidine compounds or Compounds of Formula (I), processes for their production, their use as pharmaceuticals and pharmaceutical compositions comprising them.
    Type: Grant
    Filed: December 7, 2009
    Date of Patent: January 21, 2014
    Assignee: Intra-Cellular Therapies, Inc.
    Inventors: Peng Li, Jun Zhao, Hailin Zeng, Lawrence Wennogle
  • Publication number: 20140011783
    Abstract: Optionally substituted 4,5,7,8-tetrahydro-(optionally 4-thioxo or 4-imino)-(1H or 2H)-imidazo[1,2-a]pyrazolo[4,3-e]pyrimidine or 4,5,7,8,9-pentahydro-(optionally 4-thioxo or 4-imino)-(1H or 2H)-pyrimido[1,2-a]pyrazolo[4,3-e]pyrimidine compounds or Compounds of Formula (I), processes for their production, their use as pharmaceuticals and pharmaceutical compositions comprising them.
    Type: Application
    Filed: September 6, 2013
    Publication date: January 9, 2014
    Applicant: INTRA-CELLULAR THERAPIES, INC.
    Inventors: Peng LI, Jun ZHAO, Hailin ZHENG, Lawrence P. WENNOGLE
  • Publication number: 20140005155
    Abstract: Optionally substituted 3-(thio, sulfinyl or sulfonyl)-7,8-dihydro-(1H or 2H)-imidazo[1,2-a]pyrazolo[4,3-e]pyrimidin-4(5H)-one or a substituted 3-(thio, sulfinyl or sulfonyl)-7,8,9-trihydro-(1H or 2H)-pyrimido[1,2-a]pyrazolo[4,3-e]pyrimidin-4(5H)-one compounds or Compounds of Formula (I), processes for their production, their use as pharmaceuticals and pharmaceutical compositions comprising them.
    Type: Application
    Filed: September 6, 2013
    Publication date: January 2, 2014
    Applicant: INTRA-CELLULAR THERAPIES, INC
    Inventors: Peng LI, Jun ZHAO, Hailin ZHENG, Lawrence P. WENNOGLE
  • Publication number: 20140005207
    Abstract: The present invention relates to the use of a compound, suitable for modulating the interaction between first and second partner proteins, or between homologues, mutants, or fragments of said proteins, said first and second proteins being SASPase and filaggrin-2, or FLG2, as an active agent for treating and/or preventing aesthetic defects in the skin, and/or in the appendages thereof, linked to an imbalance in the differentiation and/or proliferation of the cells of the epidermis.
    Type: Application
    Filed: December 5, 2011
    Publication date: January 2, 2014
    Applicant: L'OREAL
    Inventors: Dominique Bernard, Agnes Thomas-Collignon, Roger Rozot, Benoit Muller
  • Publication number: 20130338139
    Abstract: Described herein are compounds of Formula I and Formula II, methods of their synthesis, compositions comprising the compounds, and use of the compounds and compositions in treating numerous diseases and disorders, including cognitive deficits associated with CNS diseases and disorders.
    Type: Application
    Filed: June 18, 2013
    Publication date: December 19, 2013
    Inventors: Amy Allan, Bryan Branstetter, James Breitenbucher, Brian Dyck, Tawfik Gharbaoui, Laurent Gomez, Andrew Richard Hudson, Tami Jo Marrone, Troy Vickers, Michael I. Weinhouse
  • Publication number: 20130331376
    Abstract: The present invention provides compounds having a structure according to Formula (I): or a salt or solvate thereof, wherein ring A, E1, E2, R1, R2, R3 and R4 are defined herein. The invention further provides pharmaceutical compositions including the compounds of the invention and methods of making and using the compounds and compositions of the invention, e.g., in the treatment and prevention of various disorders, such as Parkinson's disease.
    Type: Application
    Filed: August 14, 2013
    Publication date: December 12, 2013
    Applicant: Elan Corporation, Inc.
    Inventors: Robert A. Galemmo, Dean R. Artis, Michael Ye, Danielle Aubele, Anh Truong, Simeon Bowers, Roy K. Hom, Yong-Liang Zhu, R. Jeffrey Neitz, Jennifer Sealy, Marc Adler, Paul Beroza, John P. Anderson
  • Publication number: 20130331363
    Abstract: Optionally substituted (1- or 3-oxy)-4,5,7,8-tetrahydro-(optionally 4-oxo, 4-thioxo or 4-imino)-2H-imidazo[1,2-a]pyrrolo[3,4-e]pyrimidine or (1- or 3-oxy)-4,5,7,8,9-pentahydro-(optionally 4-oxo, 4-thioxo or 4-imino)-2H-pyrimido[1,2-a]pyrrolo[3,4-e]pyrimidine compounds, processes for their production, their use as pharmaceuticals and pharmaceutical compositions comprising the same.
    Type: Application
    Filed: May 31, 2011
    Publication date: December 12, 2013
    Applicant: INTRA-CELLULAR THERAPIES, INC.
    Inventors: Peng Li, Jun Zhao
  • Publication number: 20130324723
    Abstract: Provided are tetraazapyrene compounds of formula (I) and their use as n-type semiconductors. In formula (I), R1, R2, R3, R4, at each occurrence, independently are selected from H, a C1-30 alkyl group, a C1-30 alkoxy group, a C1-30 alkylthio group, a C6-14 aryl group, a C6-14 aryloxy group, a C6-14 arylthio group, a C7-20 arylalkyl group, CI and Br; R5, R6, at each occurrence, independently are selected from H, a C1-30 alkyl group, a Cy1-30 haloalkyl group, a C6-14 aryl group and a C7-20 arylalkyl group, wherein aryl and arylalkyl can be optionally substituted with one or more halogen, C1-4 haloalkyl, —CN, —NO2, —CHO, —COOH, —CONH2, —CO(C1-14 alkyl), —COO(C1-14 alkyl), CONHC(C1-14 alkyl) and —CON(C1-14 alkyl)2 groups, with the proviso that at least one of R1, R2, R3, R4 is a C6-14 aryloxy, a C6-14 arylthio I group, CI or Br. (I).
    Type: Application
    Filed: February 16, 2012
    Publication date: December 5, 2013
    Applicant: BASF SE
    Inventors: Nicolle Langer, Sonja Geib, Susanne Martens, Lutz Gade
  • Patent number: 8598342
    Abstract: The present invention provides Wall Teichoic Acid biosynthesis inhibitors such as compound 1835F03 (targocil) and related synthetic analogs. The invention also provides pharmaceutical compositions thereof and methods for treating bacterial infection and the suppression of growth of bacterial cells by administering a Wall Teichoic Acid biosynthesis inhibitor. The invention is particularly useful for the treatment of Methicillin-resistant Staphylococcus aureus (MRSA). The invention further provides procedures for the syntheses of Wall Teichoic Acid biosynthesis inhibitors. The invention also provides methods for the identification of antibacterial therapeutic agents.
    Type: Grant
    Filed: June 5, 2009
    Date of Patent: December 3, 2013
    Assignee: President and Fellows of Harvard College
    Inventors: Suzanne Walker Kahne, Jonathan G. Swoboda, Timothy C. Meredith, Kyungae Lee, Jennifer Campbell
  • Publication number: 20130306955
    Abstract: A specific nitrogen-containing heterocyclic compound having a urea structure, an electron transporting material containing the nitrogen-containing heterocyclic compound, and an organic electroluminescence device including a light emitting layer and an electron transporting layer between a cathode and an anode in which the electron transporting layer includes the electron transporting material or the nitrogen-containing heterocyclic derivative. An organic EL device exhibiting high emission efficiency even at low voltage and a material for organic EL devices are described.
    Type: Application
    Filed: February 1, 2012
    Publication date: November 21, 2013
    Applicant: IDEMITSU KOSAN CO., LTD.
    Inventors: Sayaka Mizutani, Takayasu Sado, Hiroki Ishida
  • Publication number: 20130302416
    Abstract: New substituted tricyclic compounds of formula (I) are described, wherein R1, R2, X, Y, Z are herein defined, having protein kinase inhibiting activity. The invention includes methods to prepare the compounds of formula (I), pharmaceutical compositions containing them, and their use in therapy, in particular for the treatment of diseases caused by and/or associated with dysregulated activity of protein kinase.
    Type: Application
    Filed: January 19, 2012
    Publication date: November 14, 2013
    Applicant: NERVIANO MEDICAL SCIENCES S.R.L.
    Inventors: Marina Caldarelli, Francesco Casuscelli, Daniele Donati, Danilo Mirizzi, Francesca Quartieri, Marco Silvagni
  • Publication number: 20130285036
    Abstract: The present invention relates to aromatic nitrogen heterocycles, and to electronic devices, in particular organic electroluminescent devices, which comprise these aromatic nitrogen heterocycles, in particular in a hole-injection layer and/or in a hole-transport layer and/or in a hole-blocking layer and/or in an electron-transport layer and/or in an emitting layer.
    Type: Application
    Filed: December 15, 2011
    Publication date: October 31, 2013
    Applicant: MERCK PATENT GMBH
    Inventors: Philipp Stoessel, Arne Buesing, Esther Breuning, Christof Pflumm, Amir Hossain, Thomas Eberle, Teresa Mujica-Fernaud
  • Patent number: 8546513
    Abstract: The disclosure relates to methods and materials useful for polymerizing a monomer. In one embodiment, for example, the disclosure provides a method for polymerizing a monomer containing a plurality of electrophilic groups, wherein the method comprises contacting the monomer with a nucleophilic reagent in the presence of a guanidine-containing catalyst. The methods and materials of the disclosure find utility, for example, in the field of materials science.
    Type: Grant
    Filed: January 7, 2013
    Date of Patent: October 1, 2013
    Assignees: International Business Machines Corporation, The Board of Trustees of the Leland Stanford Junior University
    Inventors: James L. Hedrick, Russell C. Pratt, Robert M. Waymouth
  • Patent number: 8536159
    Abstract: Optionally substituted 3-(thio, sulfonyl or sulfonyl)-7,8-dihydro-(1H or 2H)-imidazo[1,2-a]pyrazolo[4,3-e]pyrimidin-4(5H)-one or a substituted 3-(thio, sulfinyl or sulfonyl)-7,8,9-trihydro-(1H or 2H)-pyrimido[1,2-a]pyrazolo[4,3-e]pyrimidin-4(5H)-one compounds or Compounds of Formula (I), processes for their production, their use as pharmaceuticals and pharmaceutical compositions comprising them.
    Type: Grant
    Filed: December 7, 2009
    Date of Patent: September 17, 2013
    Assignee: Intra-Cellular Therapies, Inc.
    Inventors: Peng Li, Jun Zhao, Hailin Zeng, Lawrence Wennogle
  • Publication number: 20130217675
    Abstract: This disclosure is directed to pyrido[4,3-b]indole and pyrido[3,4-b]indole derivatives. Pharmaceutical compositions comprising the compounds are also provided, as are methods of using the compounds in a variety of therapeutic applications, including the treatment of a cognitive disorder, psychotic disorder, neurotransmitter-mediated disorder and/or a neuronal disorder.
    Type: Application
    Filed: February 18, 2011
    Publication date: August 22, 2013
    Inventors: Sarvajit Chakravarty, Barry Patrick Hart, Rajendra Parasmal Jain
  • Patent number: 8513436
    Abstract: Disclosed herein are novel antioxidant inflammation modulators, including those of the formula: wherein the variables are defined herein. Also provided are pharmaceutical compositions, kits and articles of manufacture comprising such compounds. Methods and intermediates useful for making the compounds, and methods of using the compounds and compositions thereof are also provided.
    Type: Grant
    Filed: December 19, 2011
    Date of Patent: August 20, 2013
    Assignee: Reata Pharmaceuticals, Inc.
    Inventors: Eric Anderson, Gary L. Bolton, Bradley Caprathe, Xin Jiang, Chitase Lee, William H. Roark, Melean Visnick
  • Publication number: 20130207048
    Abstract: The present invention relates to compounds of the formula (I), to the use of the compounds in electronic devices, to processes for the preparation of the compounds, and to electronic devices comprising the compounds, preferably as electron-transport materials, as hole-blocking materials, as matrix materials and/or as emitter materials.
    Type: Application
    Filed: September 8, 2011
    Publication date: August 15, 2013
    Applicant: Merck Patent GmbH Patents & Scientific Information
    Inventors: Jochen Schwaiger, Heinrich Becker
  • Patent number: 8492504
    Abstract: The disclosure relates to methods and materials useful for depolymerizing a polymer. In one embodiment, for example, the disclosure provides a method for depolymerizing a polymer containing electrophilic linkages, wherein the method comprises contacting the polymer with a nucleophilic reagent in the presence of a guanidine-containing compound. The methods and materials of the disclosure find utility, for example, in the field of waste reclamation and recycling.
    Type: Grant
    Filed: August 7, 2012
    Date of Patent: July 23, 2013
    Assignees: International Business Machines Corporation, The Board of Trustees of the Leland Stanford Junior University
    Inventors: James Lupton Hedrick, Russell Clayton Pratt, Robert M. Waymouth
  • Patent number: 8486901
    Abstract: Novel sodium channel blocking compounds tetrodotoxm galactopyranosides of formula I were isolated and purified by HPLC and identified further through IR, NMR, GC, and MS. The compounds have a galactopyranosyl moiety attached to C11 of tetrodotoxin and retain the analgesic activity of the latter. Pharmaceutical compositions and medical uses thereof are further disclosed.
    Type: Grant
    Filed: March 26, 2010
    Date of Patent: July 16, 2013
    Assignee: Wex Medical Limited
    Inventor: Weiyang Lin
  • Publication number: 20130172320
    Abstract: This disclosure is directed to pyrido[4,3-b]indole and pyrido[3,4-b]indole derivatives. Pharmaceutical compositions comprising the compounds are also provided, as are methods of using the compounds in a variety of therapeutic applications, including the treatment of a cognitive disorder, psychotic disorder, neurotransmitter-mediated disorder and/or a neuronal disorder.
    Type: Application
    Filed: February 18, 2011
    Publication date: July 4, 2013
    Inventors: Sarvajit Chakravarty, Barry Patrick Hart, Rajendra Parasmal Jain
  • Publication number: 20130156851
    Abstract: What is described are macrocyclic compounds formed by reaction of a cyclic compound, which contains an amine, with an epoxide. The macrocyclic compound has the following structure: When substituents R and R? that are hydrophobic substituents, the macrocyclic compound functions as a lipid and is compatible with lipid systems, including liposomes and lipid particles. When present in certain lipid systems, the macrocyclic compound enhances the ability of the lipid system to facilitate delivery of therapeutic molecules to target cells in a mammalian subject.
    Type: Application
    Filed: August 26, 2011
    Publication date: June 20, 2013
    Inventors: Kunyuan Cui, Dong Liang