Three Or More Ring Hetero Atoms In The Tetracyclo Ring System Patents (Class 546/64)
  • Patent number: 11322693
    Abstract: Disclosed is an organic light-emitting device using a compound capable of emitting delayed fluorescence and capable of undergoing intramolecular hydron transfer. The compound includes, for example, a compound represented by the general formula. X1 to X3 each represent O or S; R1 to R6 each represent nH or a substituent; n, n1 to n3 each represent an integer of 1 to 3.
    Type: Grant
    Filed: December 20, 2017
    Date of Patent: May 3, 2022
    Assignees: KYUSHU UNIVERSITY NATIONAL UNIVERSITY CORPORATION, KYULUX, INC.
    Inventors: Masashi Mamada, Chihaya Adachi, Hajime Nakanotani, YuSeok Yang
  • Patent number: 11046693
    Abstract: The invention relates to novel pyrido-phenanthroline derivatives, to the production and use thereof in the field of medicine, in particular for cancer therapy.
    Type: Grant
    Filed: November 24, 2017
    Date of Patent: June 29, 2021
    Assignee: CHRISTIAN-ALBRECHTS-UNIVERSITÄT ZU KIEL
    Inventors: Bernd Clement, Christopher Meier, Tamara Natalie Steinhauer
  • Patent number: 11040973
    Abstract: The present invention generally relates to compounds as a dual kinase-demethylase inhibitor useful for the treatment of diseases mediated by a kinase and/or a histone demethylase, such as inflammation, cancer, viral and bacterial infections, neurological and immunological disorders. Pharmaceutical compositions and methods for treating those diseases are within the scope of this invention.
    Type: Grant
    Filed: March 29, 2018
    Date of Patent: June 22, 2021
    Inventors: Herman O. Sintim, Neetu Dayal, Clement Opoku-Temeng
  • Patent number: 10654854
    Abstract: The disclosure provides new, stable, pharmaceutically acceptable salt forms of 1-(4-fluoro-phenyl)-4-((6bR,10aS)-3-methyl-2,3,6b,9,10,10a-hexahydro-1H,7H-pyrido[3?,4?:4,5]pyrrolo[1,2,3-de]quinoxalin-8-yl)-butan-1-one, together with methods of making and using them, and pharmaceutical compositions comprising them.
    Type: Grant
    Filed: March 28, 2017
    Date of Patent: May 19, 2020
    Assignee: INTRA-CELLULAR THERAPIES, INC.
    Inventors: Peng Li, Edwin Aret
  • Patent number: 10399979
    Abstract: The invention described herein pertains to selective Janus kinase (JAK) inhibitors and methods of use thereof. Also described are methods for treating diseases involved abnormal JAK/STAT signaling pathway in mammals using the described selective JAK inhibitors or a pharmaceutical formulation thereof.
    Type: Grant
    Filed: October 31, 2018
    Date of Patent: September 3, 2019
    Assignee: Purdue Research Foundation
    Inventors: Mark Stanley Cushman, Mohamed S. A. Elsayed
  • Patent number: 10115908
    Abstract: Disclosed is an imidazole[4,5-f][1,10]phenanthroline derivative conforming to the chemical structural formula of: Wherein X and Y are independently selected from the group consisting of Z-substituted aryl ring, Z-substituted heteroaryl ring, unsubstituted aryl ring, or unsubstituted heteroaryl ring, and wherein Z is independently selected from the group consisting of aryl, C1-4 alkoxy, amino, nitro, trifluoromethyl, cyano, halo atom, or C1-24 aliphatic hydrocarbyl. The present invention further discloses a method of preparing the imidazole[4,5-f][1,10]phenanthroline derivative and the use thereof.
    Type: Grant
    Filed: August 22, 2014
    Date of Patent: October 30, 2018
    Assignee: BOE Technology Group Co., Ltd.
    Inventor: Juanjuan You
  • Patent number: 10100055
    Abstract: There is provided a production method for the purpose of improving the solubility of an arginine-residue imidazopyrroloquinoline in water and making the purity thereof high. There is provided a compound represented by general formula (1): wherein n is 1, 2, 3 or 4; and M is an alkali metal or ammonium.
    Type: Grant
    Filed: December 18, 2017
    Date of Patent: October 16, 2018
    Assignee: MITSUIBISHI GAS CHEMICAL COMPANY, INC.
    Inventor: Kazuto Ikemoto
  • Patent number: 9822113
    Abstract: The present invention relates to novel tricyclic compounds of formula (I) and (II) More particularly, the present invention relates to novel tricyclic compounds of formula (I) and (II) and process of preparation of these compounds from 4,5-di-methyl-o-phenylinediamine. Further, the present invention relates to a process for preparation of tricyclic compound hunanamycin A.
    Type: Grant
    Filed: July 14, 2014
    Date of Patent: November 21, 2017
    Assignee: Council of Scientific & Industrial Research
    Inventors: Dumbala Srinivasa Reddy, Rahul Dilip Shingare, Velayudham Ramadoss
  • Patent number: 9034486
    Abstract: A triazole derivative represented by General Formula (G0) is provided. In the General formula (G0), A represents a substituted or unsubstituted carbazolyl group, a substituted or unsubstituted dibenzothiophenyl group, or a substituted or unsubstituted dibenzofuranyl group, E represents substituted or unsubstituted triazolo [4,3 f]phenanthridine or substituted or unsubstituted triazolo [3,4-?]isoquinoline, and Ar represents a substituted or unsubstituted arylene group having 6 to 13 carbon atoms.
    Type: Grant
    Filed: July 29, 2011
    Date of Patent: May 19, 2015
    Assignee: SEMICONDUCTOR ENERGY LABORATORY CO., LTD
    Inventors: Hiroshi Kadoma, Yuko Kawata, Nobuharu Ohsawa, Satoshi Seo
  • Patent number: 9018227
    Abstract: The invention provides novel nicotinic acetylcholine receptor agonists, for example, phantasmidine and derivatives thereof, for example a compound of formula (I). Also disclosed are methods of treating disorders responsive to nicotinic acetylcholine receptor agonists such as Alzheimer's disease, schizophrenia, Myasthenia Gravis, Tourette's syndrome, Parkinson's disease, epilepsy, pain, and cognitive dysfunction by treatment with the nicotinic acetylcholine for agonists.
    Type: Grant
    Filed: March 18, 2011
    Date of Patent: April 28, 2015
    Assignees: Indiana State University, The United States of America, as Represented by the Secretary, Department of Health and Human Services
    Inventors: Richard W. Fitch, Thomas F. Spande, H. Martin Garraffo, Herman J. C. Yeh, Kathryn Daly
  • Publication number: 20150099774
    Abstract: New phenanthroline derivatives as drug as well as methods for producing said compounds are provided.
    Type: Application
    Filed: April 5, 2013
    Publication date: April 9, 2015
    Inventors: Bernd Clement, Christopher Meier, Dieter Heber, Lars Stenzel
  • Patent number: 8993588
    Abstract: Compounds of formula I: wherein variables A1, A2, B, m, n, J, R4, G1, G2, G3 and Y are as described herein, which are antagonists of CGRP receptors and which are useful in the treatment or prevention of diseases in which the CGRP is involved, such as migraine. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which CGRP is involved.
    Type: Grant
    Filed: June 2, 2008
    Date of Patent: March 31, 2015
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Ian Bell, Harold Selnick, C. Blair Zartman
  • Publication number: 20150080366
    Abstract: Compounds of Formula (I) wherein n, A, R1, R2, R3 and R5 are defined herein, are useful for the treatment of cytomegalovirus disease and/or infection.
    Type: Application
    Filed: April 3, 2013
    Publication date: March 19, 2015
    Applicant: Boehringer Ingelheim International GmbH
    Inventors: Lee Fader, Pierre Louis Beaulieu, Murray Bailey, Francois Bilodeau, Rebekah J. Carson, André Giroux, Cédrickx Godbout, Oliver Hucke, Marc-André Joly, Mélissa Leblanc, Olivier Lepage, Benoit Moreau, Julie Naud, Martin Poirier, Elisia Villemure
  • Patent number: 8962620
    Abstract: The present invention relates to substituted 6,5-fused bicyclic heteroaryl compounds. The present invention also relates to pharmaceutical compositions containing these compounds and methods of treating cancer by administering these compounds and pharmaceutical compositions to subjects in need thereof.
    Type: Grant
    Filed: November 4, 2013
    Date of Patent: February 24, 2015
    Assignee: Epizyme, Inc.
    Inventors: Kevin Wayne Kuntz, Edward James Olhava, Richard Chesworth, Kenneth William Duncan
  • Patent number: 8940896
    Abstract: In accordance with the present invention, tetracyclic caboline derivatives that inhibit the expression of VEGF post-transcriptionally have been identified, and methods for their use provided. In one aspect of the invention, these compounds useful in the inhibition of VEGF production, in the inhibition of angiogenesis, and/or in the treatment of cancer, diabetic retinopathy or exudative macular degeneration are provided. In another aspect of the invention, methods are provided for the inhibition of VEGF production, the inhibition of angiogenesis, and/or the treatment of cancer, diabetic retinopathy or exudative macular degeneration using the compounds of the invention.
    Type: Grant
    Filed: March 15, 2005
    Date of Patent: January 27, 2015
    Assignee: PTC Therapeutics, Inc.
    Inventors: Young-Choon Moon, Liangxian Cao, Nadarajan Tamilarasu, Hongyan Qi, Soongyu Choi, William Joseph Lennox, Donald Thomas Corson
  • Patent number: 8927566
    Abstract: The present invention relates to a norepinephrine and selective serotonin receptor blocker and the use thereof. The norepinephrine and selective serotonin receptor blocker is a compound of formula I, or isomers, pharmaceutically acceptable salts or solvates thereof, wherein R1 is selected from the group consisting of C1-6 alkyl, C1-6 alkoxy, C6-10 aralkyl, C6-10 arylalkoxy, C1-6 haloalkyl and C1-6 haloalkoxy; and R2 is one or more groups each independently selected from the group consisting of hydrogen, halogen, C1-6 alkyl, C1-6 alkoxy, nitro, cyano, amino, hydroxyl, C1-6 haloalkyl, and C1-6 haloalkoxy. R3 is one or more groups each independently selected from the group consisting of hydrogen, halogen, C1-6 alkyl, C1-6 alkoxy, nitro, cyano, amino, hydroxyl, C1-6 haloalkyl, and C1-6 haloalkoxy. The compound of the present invention is effective norepinephrine and selective serotonin receptor blocker.
    Type: Grant
    Filed: November 21, 2012
    Date of Patent: January 6, 2015
    Assignee: Beijing Medisan Technology Co., Ltd.
    Inventors: Mingxin Wang, Jinai Liu, Fan Yang, Ailing Wang, Jiguo Sun, Yan Wang, Jin Cui, Lei Ji
  • Publication number: 20140361259
    Abstract: An arylamine-based compound is represented by Formula 1 below. The arylamine-based compound is included in an organic light emitting diode.
    Type: Application
    Filed: October 23, 2013
    Publication date: December 11, 2014
    Applicant: SAMSUNG DISPLAY CO., LTD.
    Inventors: Seok-Hwan Hwang, Young-Kook Kim, Hye-Jin Jung, Jun-Ha Park, Eun-Young Lee, Jin-O Lim, Sang-Hyun Han, Eun-Jae Jeong, Soo-Yon Kim, Jong-Hyuk Lee
  • Patent number: 8895726
    Abstract: The present invention relates to a compound derived from indole corresponding to the following formula II: wherein X represents N, CR8 or N+R8, wherein R8 represents a hydrogen atom, a hydroxyl or alkyl or methoxy group optionally substituted with a phenyl group; R2, R3 and R4 independently represent a hydrogen atom or a halogen atom or an optionally substituted alkyl, amine, alkene, ester, sulfonamide, ether or benzyl group; R5 represents a hydrogen atom or an optionally substituted, saturated or unsaturated alkyl group, amine, benzyl group; R6 represents an optionally substituted C1-C3 alkyl group; R7 represents a hydrogen atom or an optionally substituted C1-C3 alkyl group and R7 is absent when the ring A is in the b position, and A represents a ring; R9 and R10 represent together a carbon bond or independently represent an R11 OR11, SR11 group; wherein R11 represents a hydrogen atom, an optionally substituted, saturated or unsaturated, C1-C3 alkyl group, which may contain one or more sulfur, oxygen or
    Type: Grant
    Filed: February 19, 2008
    Date of Patent: November 25, 2014
    Assignees: The Institut Curie, The University of Montpellier 2 Science and Techniques
    Inventors: Fabrice Lejeune, Jamal Tazi, David Grierson, Christian Rivalle, Florence Mahuteau-Betzer
  • Publication number: 20140343089
    Abstract: The present invention relates to a norepinephrine and selective serotonin receptor blocker and the use thereof. The norepinephrine and selective serotonin receptor blocker is a compound of formula I, or isomers, pharmaceutically acceptable salts or solvates thereof, wherein R1 is selected from the group consisting of C1-6 alkyl, C1-6 alkoxy, C6-10 aralkyl, C6-10 arylalkoxy, C1-6 haloalkyl and C1-6 haloalkoxy; and R2 is one or more groups each independently selected from the group consisting of hydrogen, halogen, C1-6 alkyl, C1-6 alkoxy, nitro, cyano, amino, hydroxyl, C1-6 haloalkyl, and C1-6 haloalkoxy. R3 is one or more groups each independently selected from the group consisting of hydrogen, halogen, C1-6 alkyl, C1-6 alkoxy, nitro, cyano, amino, hydroxyl, C1-6 haloalkyl, and C1-6 haloalkoxy. The compound of the present invention is effective norepinephrine and selective serotonin receptor blocker.
    Type: Application
    Filed: November 21, 2012
    Publication date: November 20, 2014
    Inventors: Mingxin Wang, Jinai Liu, Fan Yang, Ailing Wang, Jiguo Sun, Yan Wang, Jin Cui, Lei Ji
  • Publication number: 20140302987
    Abstract: Use of substituted isoquinolinones, isoquinolinediones, isoquinolinetriones and dihydroisoquinolinones of the general formula (I) or their respective salts where the radicals in the general formula (I) correspond to the definitions given in the description, for enhancing stress tolerance in plants to abiotic stress, for strengthening plant growth and/or for increasing plant yield, and selected processes for preparing the compounds mentioned above.
    Type: Application
    Filed: July 2, 2012
    Publication date: October 9, 2014
    Applicant: BAYER INTELLECTUAL PROPERTY GmbH
    Inventors: Jens Frackenpohl, Hans-Joachim Zeiss, Ines Heinemann, Lothar Willms, Thomas Müller, Marco Busch, Pascal Von Koskull-Döering, Christopher Hugh Rosinger, Jan Dittgen, Martin Jeffrey Hills
  • 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: 8853234
    Abstract: The present invention provides novel quinolone compounds and pharmaceutical composition thereof which may inhibit cell proliferation and/or induce cell apoptosis. The present invention also provides methods of preparing such compounds and compositions, and methods of making and using the same.
    Type: Grant
    Filed: March 9, 2011
    Date of Patent: October 7, 2014
    Assignee: Senhwa Biosciences, Inc.
    Inventors: Johnny Yasuo Nagasawa, Fabrice Pierre, Mustapha Haddach, Michael Schwaebe, Levan Darjania, Jeffrey P. Whitten
  • Patent number: 8829023
    Abstract: The invention relates to a process for obtaining compounds derived from tetrahydro-?-carboline, specifically tadalafil and intermediate products from the synthesis, comprising the reaction between piperonal and an alkyl ester of D-tryptophan as a salt, and in the absence of any other component, followed by haloacetylation and a final cyclization with methylamine.
    Type: Grant
    Filed: February 10, 2012
    Date of Patent: September 9, 2014
    Assignee: Interquim, S.A.
    Inventors: Xavier Berzosa Rodríguez, Francisco Marquillas Olondriz
  • Publication number: 20140225088
    Abstract: A compound for an organic optoelectronic device represented by Chemical Formula 1 wherein, in Chemical Formula 1, variables A, Y1 to Y4, X1, m, R1 to R4, L1 to L3, n1 to n3, Ar1 and Ar2 are described in the specification.
    Type: Application
    Filed: February 10, 2014
    Publication date: August 14, 2014
    Applicants: CHEIL INDUSTRIES INC., SAMSUNG ELECTRONICS CO., LTD.
    Inventors: Kyu Young HWANG, Sang Mo KIM, Young Kwon KIM, Joo Hee SEO, Jhun Mo SON, Yong Sik JUNG, Seok-Hwan HONG
  • 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: 20140213571
    Abstract: The present invention relates to compounds of formula (I) that are useful as hepatitis C virus (HCV) NS5B polymerase inhibitors, the synthesis of such compounds, and the use of such compounds for inhibiting HCV NS5B polymerase activity, for treating or preventing HCV infections and for inhibiting HCV viral replication and/or viral production in a cell-based system.
    Type: Application
    Filed: August 20, 2012
    Publication date: July 31, 2014
    Inventors: Nigel J. Liverton, Casey Cameron McComas, Joerg Habermann, Uwe Koch, Frank Narjes, Peng Li, Xuanjia Peng, Richard Soll, Hao Wu, Anandan Palani, Shuwen He, Xing Dai, Hong Liu, Zhong Lai, Clare London, Dong Xiao, Nicolas Zorn, Ravi Nargund
  • Publication number: 20140162985
    Abstract: The invention provides a compound of Formula (I) pharmaceutically acceptable salts, pro-drugs, biologically active metabolites, stereoisomers and isomers thereof wherein the variable are defined herein. The compounds of the invention are useful for treating immunological and oncological conditions.
    Type: Application
    Filed: September 6, 2013
    Publication date: June 12, 2014
    Applicant: ABBVIE INC.
    Inventors: Andrew Burchat, Thomas D. Gordon, Kelly D. Mullen, David C. Ihle, Michael J. Morytko, Kevin P. Cusack, Gloria Y. Lo Schiavo, Lei Wang, Michael Friedman
  • Patent number: 8664396
    Abstract: A method of staining a poly(amino acid) by contacting a poly(amino acid) with an overall neutral or overall cationic complex of at least one of transition metal ion, and a plurality of donor ligands each of which is fully coordinated to the transition metal ion and is either a nitrogen donor ligand or a cyclometalated donor ligand, such that at least one of the donor ligands is a cyclometalated donor ligand. Nitrogen donor ligands will contain heteroaryl ring systems having from 10 to 40 ring atoms, wherein each nitrogen donor ligand is substituted with from 0 to 4 R1 groups. Cyclometalated donor ligands will likewise contain heteroaryl ring systems having from 10 to 40 ring atoms, such that at least one ring atom is N, wherein each cyclometalated donor ligand is substituted with from 0 to 4 R1 groups. R1, R2, R3 and R4 groups are defined herein.
    Type: Grant
    Filed: November 20, 2008
    Date of Patent: March 4, 2014
    Assignee: Bio-Rad Laboratories, Inc.
    Inventor: Tom Berkelman
  • Publication number: 20140031544
    Abstract: The present invention relates to compounds defined by formula I wherein the variables R1, R2, R3, R4, and m are defined as in claim 1, possessing valuable pharmacological activity. Particularly, the compounds are inhibitors of 11?-hydroxysteroid dehydrogenase (HSD) 1 and thus are suitable for treatment and prevention of diseases which can be influenced by inhibition of this enzyme, such as metabolic diseases, in particular diabetes type 2, obesity, and dyslipidemia.
    Type: Application
    Filed: June 20, 2013
    Publication date: January 30, 2014
    Applicants: Boehringer Ingelheim International GmbH, Vitae Pharmaceuticals, Inc.
    Inventors: Matthias Eckhardt, Frank Himmelsbach, Linghang Zhuang, Stefan Peters, Herbert Nar
  • Publication number: 20140031362
    Abstract: The present invention relates to compounds of following general formula (I): and to the pharmaceutically acceptable salts of same, the tautomers of same, the stereoisomers or mixture of stereoisomers in any proportions of same, such as a mixture of enantiomers, notably a racemic mixture, as well as to methods for preparing same and uses of same, notably as an antineoplastic agent.
    Type: Application
    Filed: April 12, 2012
    Publication date: January 30, 2014
    Applicant: PIERRE FABRE MEDICAMENT
    Inventors: Rémi Rabot, Karim Bedjeguelal, El Bachir Kaloun, Philippe Schmitt, Nicolas Rahier, Patrice Mayer, Emmanuel Fournier
  • Patent number: 8598167
    Abstract: The present invention relates to substituted 6,5-fused bicyclic heteroaryl compounds. The present invention also relates to pharmaceutical compositions containing these compounds and methods of treating cancer by administering these compounds and pharmaceutical compositions to subjects in need thereof.
    Type: Grant
    Filed: July 9, 2013
    Date of Patent: December 3, 2013
    Assignee: Epizyme, Inc.
    Inventors: Kevin Wayne Kuntz, Edward James Olhava, Richard Chesworth, Kenneth William Duncan
  • Patent number: 8580956
    Abstract: In its many embodiments, the present invention provides a novel class of heterocyclic compounds as modulators of gamma secretase, 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 diseases associated with the central nervous system using such compounds or pharmaceutical compositions.
    Type: Grant
    Filed: May 28, 2008
    Date of Patent: November 12, 2013
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Zhaoning Zhu, William J. Greenlee, Zhong-Yue Sun, Gioconda Gallo, Ruo Xu, Xianhai Huang, Xiaohong Zhu
  • Publication number: 20130296307
    Abstract: Provided herein are compounds according to Formula I and pharmaceutically acceptable salts thereof, and compositions comprising the same, for use in various methods, including treating cancers such as colon, ovarian, pancreatic, breast, liver, prostate and hematologic cancers:
    Type: Application
    Filed: July 10, 2013
    Publication date: November 7, 2013
    Inventors: John Hood, Sunil Kumar KC, David Mark Wallace
  • Publication number: 20130281482
    Abstract: The invention provides novel nicotinic acetylcholine receptor agonists, for example, phantasmidine and derivatives thereof, for example a compound of formula (I). Also disclosed are methods of treating disorders responsive to nicotinic acetylcholine receptor agonists such as Alzheimer's disease, schizophrenia, Myasthenia Gravis, Tourette's syndrome, Parkinson's disease, epilepsy, pain, and cognitive dysfunction by treatment with the nicotinic acetylcholine for agonists.
    Type: Application
    Filed: March 18, 2011
    Publication date: October 24, 2013
    Applicant: The United States of America, as represented by Secretary, Department of Health and Human Services
    Inventor: Kathryn Daly
  • Patent number: 8557991
    Abstract: Disclosed is a novel process for the preparation of pharmacologically interesting indolopyridine derivatives containing tetracyclic tetrahydro-11-carboline-hydantoines linked to a basic side chain and the corresponding salts, which can be used as Eg5 inhibitors, with very high overall chemical yield and enantiomeric purity.
    Type: Grant
    Filed: March 5, 2009
    Date of Patent: October 15, 2013
    Assignee: 4SC AG
    Inventors: Bernd Muller, Helmut Schlemper
  • Publication number: 20130225558
    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: Application
    Filed: February 18, 2011
    Publication date: August 29, 2013
    Inventors: Sarvajit Chakravarty, Barry Patrick Hart, Rajendra Parasmal Jain
  • 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
  • Publication number: 20130200339
    Abstract: A heterocyclic compound includes a compound represented by Formula 1.
    Type: Application
    Filed: October 2, 2012
    Publication date: August 8, 2013
    Applicant: SAMSUNG DISPLAY CO., LTD.
    Inventor: Samsung Display Co., Ltd.
  • Publication number: 20130190344
    Abstract: This disclosure relates to new heterocyclic compounds that may be used to modulate a histamine receptor in an individual. Pyrido[4,3-b]indoles are described, as are pharmaceutical compositions comprising the compounds and 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: March 8, 2013
    Publication date: July 25, 2013
    Applicant: MEDIVATION TECHNOLOGIES, INC.
    Inventor: MEDIVATION TECHNOLOGIES, INC.
  • Publication number: 20130184304
    Abstract: This disclosure relates to new heterocyclic compounds that may be used to modulate a histamine receptor in an individual. Pyrido[4,3-b]indoles are described, as are pharmaceutical compositions comprising the compounds and 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: March 8, 2013
    Publication date: July 18, 2013
    Applicant: Medivation Technologies, Inc.
    Inventor: Medivation Technologies, Inc.
  • Publication number: 20130184303
    Abstract: This disclosure relates to new heterocyclic compounds that may be used to modulate a histamine receptor in an individual. Pyrido[4,3-b]indoles are described, as are pharmaceutical compositions comprising the compounds and 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: March 8, 2013
    Publication date: July 18, 2013
    Applicant: MEDIVATION TECHNOLOGIES, INC.
    Inventor: Medivation Technologies, Inc.
  • 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: 8481556
    Abstract: The present invention is directed to piperidinone carboxamide azaindane derivatives which are antagonists of CGRP receptors and useful in the treatment or prevention of diseases in which the CGRP is involved, such as migraine. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which CGRP is involved.
    Type: Grant
    Filed: November 10, 2011
    Date of Patent: July 9, 2013
    Assignee: Merck, Sharp & Dohms, Corp.
    Inventors: Ian M. Bell, Mark E. Fraley
  • Publication number: 20130065875
    Abstract: The invention provides derivatives and analogues of triazatetracyclo[7.7.0.01,13,02,7]-hexadeca-2,4,6,10,12-pentaenes, 5,7,11-triazatetracyclo[8.7.0.01,6,012,17]-heptadeca-6,8,12,14,16-pentaenes, pharmaceutical compositions comprising these compounds and methods for treatment of hepatitis C viral infections using these compounds.
    Type: Application
    Filed: October 27, 2010
    Publication date: March 14, 2013
    Applicants: THE SCRIPPS RESEARCH INSTITUTE, TRUSTEES OF BOSTON UNIVERSITY
    Inventors: John K. Snyder, Wanguo Wei, Feng Ni, Arthur Donny Strosberg, Smitha Kota, Virginia Takahashi
  • Patent number: 8394815
    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: Grant
    Filed: December 22, 2010
    Date of Patent: March 12, 2013
    Assignee: Lorus Therapeutics Inc.
    Inventors: Raed H. Al-Qawasmeh, Aiping H. Young, Mario Huesca, Yoon S. Lee
  • Publication number: 20130053363
    Abstract: [Problem] To provide a compound useful as medicine having PDE4B inhibitory activity, in particular, as an active ingredient of a composition for treating or preventing schizophrenia, Alzheimer's disease, dementia, depression and the like. [Measures for Solution] The present inventors examined compounds having PDE4B inhibitory activity and found that a tricyclic or tetracyclic imidazo[1,2-a]pyridine derivative or salts thereof had a superior PDE4B inhibitory activity, thereby completing the present invention. The imidazo[1,2-a]pyridine derivative can be used as an agent for treating or preventing schizophrenia, Alzheimer's disease, dementia, depression and the like.
    Type: Application
    Filed: October 26, 2012
    Publication date: February 28, 2013
    Applicant: Astellas Pharma Inc.
    Inventor: Astellas Pharma Inc.
  • Publication number: 20130041153
    Abstract: The present invention relates to imidazole derivatives having vinyl group represented by general formula (I) which possess electron transporting character, have a high glass transition temperature (Tg), and high decomposition temperature (Td): wherein all symbols are defined as recited in the specification. The present invention also relates to a use of the imidazole derivatives having vinyl group as a guest emitter or electron transporter in luminescent elements.
    Type: Application
    Filed: February 3, 2012
    Publication date: February 14, 2013
    Inventors: Chien-Hong CHENG, He-Pei Hsu, Ho-Hsiu Chou, Yu-Han Chen, Yi-Hsiang Chen
  • Patent number: 8318938
    Abstract: Optionally substituted chromenoisoquinolines and analogs and derivatives thereof are described herein. In addition, syntheses of these compounds are described herein. In addition, uses of these compounds as dopamine receptor binding compounds are described herein.
    Type: Grant
    Filed: August 20, 2008
    Date of Patent: November 27, 2012
    Assignee: Purdue Research Foundation
    Inventors: David Nichols, Val J. Watts
  • Publication number: 20120295882
    Abstract: This application relates to tricyclic compounds of Formula I: including all stereoisomers, mixtures of stereoisomers, and salts thereof. This application also relates to compositions comprising compounds of Formula I and uses therefore.
    Type: Application
    Filed: June 21, 2012
    Publication date: November 22, 2012
    Applicant: Cephalon, Inc.
    Inventors: Edward R. Bacon, Thomas R. Bailey, Derek D. Dunn, Greg A. Hostetler, Robert J. McHugh, George C. Morton, Gerard C. Rosse, Joseph M. Salvino, Babu G. Sundar, Rabindranath Tripathy
  • Patent number: 8293762
    Abstract: Heteroarylpyridinone derivatives represented by formula (I) wherein R1, R2, R3, R4, R5, and X are as defined in the specification, compositions thereof, and methods of use thereof. Particularly, there are described isoquinolinoyrrolopyridinones, pharmaceutical compositions including them and their use as therapeutic agents in the treatment of cancer and cell proliferation disorders.
    Type: Grant
    Filed: February 18, 2008
    Date of Patent: October 23, 2012
    Assignee: Nerviano Medical Sciences S.R.L.
    Inventors: Ermes Vanotti, Maria Menichincheri, Alessandra Scolaro