Tetracyclo Ring System Having The Diazine Ring As One Of The Cyclos (e.g., Benzophenazines, Etc.) Patents (Class 544/343)
  • Patent number: 10253254
    Abstract: The disclosure comprises novel Coelenterazine compounds and methods of use, including a simple delivery device for the photoprotein to create effects by their luminous reaction upon contact with surfaces that contain calcium. Calcium is ubiquitous in and on most surfaces and in the environment; it is this unique property of calcium that makes this a novel use of the photoproteins for entertainment. A base coelenterazine structure is depicted below.
    Type: Grant
    Filed: April 18, 2017
    Date of Patent: April 9, 2019
    Assignee: PROLUME, LTD.
    Inventors: Bruce Bryan, Hendrik Schmidt, Millard Cull
  • Patent number: 10221176
    Abstract: The present invention provides methods for the preparation of substituted heterocycle fused gamma-carbolines of Formula 2F, as shown below, intermediates useful in producing them and methods for producing such intermediates and such heterocycle fused gamma-carbolines, such methods comprising the preparation of a Compound of Formula 2F, as shown below and as further defined herein:
    Type: Grant
    Filed: July 26, 2017
    Date of Patent: March 5, 2019
    Assignee: INTRA-CELLULAR THERAPIES, INC.
    Inventors: John Charles Tomesch, Peng Li, Wei Yao, Qiang Zhang, James David Beard, Andrew S. Thompson, Hua Cheng, Lawrence P. Wennogle
  • Patent number: 9887369
    Abstract: Provided is a novel organic compound that is used as a host material in which a light-emitting substance is dispersed. The organic compound is represented by General Formula (G1). In the formula, A represents a substituted or unsubstituted dibenzofuran-diyl group, a substituted or unsubstituted dibenzothiophene-diyl group, a substituted or unsubstituted N-aryl-9H-carbazole-diyl group, or a substituted or unsubstituted N-alkyl-9H-carbazole-diyl group; Ar1 and Ar2 each independently represent a single-bond or a substituted or unsubstituted arylene group; R11 to R19 and R21 to R29 each independently represent hydrogen, an alkyl group having 1 to 6 carbon atoms, or a substituted or unsubstituted aryl group having 6 to 13 carbon atoms; X1 and X2 each independently represent a carbon atom or a nitrogen atom; and the carbon atom is bonded to hydrogen, an alkyl group having 1 to 6 carbon atoms, or a substituted or unsubstituted aryl group having 6 to 13 carbon atoms.
    Type: Grant
    Filed: August 29, 2014
    Date of Patent: February 6, 2018
    Assignee: Semiconductor Energy Laboratory Co., Ltd.
    Inventors: Yoshimi Ishiguro, Sachiko Kawakami, Hiromi Seo, Tatsuyoshi Takahashi, Satoshi Seo
  • Patent number: 9825230
    Abstract: A novel heterocyclic compound is provided. A novel heterocyclic compound that can be used for a light-emitting element is provided. A novel heterocyclic compound that can improve the reliability of a light-emitting element when used for a light-emitting element is provided. A light-emitting element, a light-emitting device, an electronic appliance, or a lighting device which includes the novel heterocyclic compound and is highly reliable is provided. One embodiment of the present invention is a heterocyclic compound represented by a general formula (G0). In the general formula (G0), A represents a dibenzo[f,h]quinoxalinyl group, B represents a substituted or unsubstituted fluorenyl group, and Ar represents a substituted or unsubstituted arylene group having 6 to 25 carbon atoms.
    Type: Grant
    Filed: April 16, 2015
    Date of Patent: November 21, 2017
    Assignee: Semiconductor Energy Laboratory Co., Ltd.
    Inventors: Hideko Inoue, Yasushi Kitano, Hiromi Seo, Tatsuyoshi Takahashi, Satoshi Seo
  • Patent number: 9751883
    Abstract: The present invention provides methods for the preparation of substituted heterocycle fused gamma-carbolines of Formula 2J, as shown below, intermediates useful in producing them and methods for producing such intermediates and such heterocycle fused gamma-carbolines, such methods comprising the preparation of a Compound of Formula 2G, as shown below, and use of said compound to produce the fused gamma-carbolines of Formula 2J, as defined herein:
    Type: Grant
    Filed: March 10, 2016
    Date of Patent: September 5, 2017
    Assignee: INTRA-CELLULAR THERAPIES, INC.
    Inventors: John Charles Tomesch, Peng Li, Wei Yao, Qiang Zhang, James David Beard, Andrew S. Thompson, Hua Cheng, Lawrence P. Wennogle
  • Patent number: 9708322
    Abstract: The invention relates to substituted heterocycle fused gamma-carbolines of the Formula Q as described herein, in free base or pharmaceutically acceptable salt form, and/or pharmaceutical compositions thereof, and methods of use in the treatment of diseases involving the 5-HT2A receptor pathway, the serotonin transporter (SERT) pathway and/or the dopamine D2 receptor pathway signaling systems.
    Type: Grant
    Filed: March 15, 2014
    Date of Patent: July 18, 2017
    Assignee: INTRA-CELLULAR THERAPIES, INC.
    Inventors: Peng Li, Qiang Zhang, Robert Davis, Lawrence P. Wennogle
  • Patent number: 9624425
    Abstract: Novel compounds in the classes of Imidazo[1,2-?]pyrazines and Imidazo[1,2-?]quinoxalines with a methoxy group modification show unique spectral properties when used as a substrate for luciferases and photo-proteins. Methoxy e-Coelenterazine an Imidazo[1,2-?] quinoxaline shifts the emission wavelength by 80 nm to blue light compared to e-Coelenterazine, using Renilla reniformis luciferase. The novel analogs described here are useful in combination with fluorescent proteins to create BRET (bioluminescent resonance energy transfer) and for other luminescent assays. In addition these novel compounds can be used in novelty items and for entertaining purposes to create different light emitting colors using the same luciferase or photoprotein.
    Type: Grant
    Filed: August 30, 2013
    Date of Patent: April 18, 2017
    Assignee: Prolume, LTD.
    Inventors: Bruce Bryan, Hendrik Schmidt, Millard Cull
  • Patent number: 9353150
    Abstract: The present application provides, among other things, a compound of Formula I-a and/or I-b, or a pharmaceutically acceptable salt thereof, wherein the variables are defined in the specification. The compounds of the invention are useful for treating various diseases including cancer.
    Type: Grant
    Filed: December 4, 2013
    Date of Patent: May 31, 2016
    Assignees: Massachusetts Institute of Technology, The Board of Trustees of the University of Illinois
    Inventors: Mohammad Movassaghi, Justin Kim, Paul J. Hergenrother, Karen Morrison, Nicolas Boyer
  • Patent number: 9315504
    Abstract: The present invention provides methods for the preparation of 4-(3-methyl-2,3,6b,9,10,10a-hexahydro-1H-pyrido-[3?,4?:4,5]-pyrrolo[1,2,3-de]quinoxalin-8-(7H)-yl)-1-(4-fluorophenyl)-1-butanone in free form or a salt thereof.
    Type: Grant
    Filed: July 3, 2014
    Date of Patent: April 19, 2016
    Assignee: INTRA-CELLULAR THERAPIES, INC.
    Inventors: John Charles Tomesch, Peng Li, Wei Yao, Qiang Zhang, James David Beard, Andrew S. Thompson, Hua Cheng, Lawrence P. Wennogle
  • Patent number: 9278970
    Abstract: The present invention relates to co-crystals of tadalafil with hydroxyl-substituted benzoic acid coformers having the following structure. Said co-crystals can be used to produce a pharmaceutical composition containing the same as the useful active ingredient. Said co-crystals can exhibit a constant storage stability.
    Type: Grant
    Filed: July 6, 2013
    Date of Patent: March 8, 2016
    Assignee: Laboratorios Senosiain S.A. de C.V.
    Inventors: Dea Herrera Ruiz, Karina Mondragón Vásquez, Hugo Morales Rojas, Herbert Höpfl, Juan Pablo Senosiain Peláez
  • Patent number: 9199995
    Abstract: The present invention relates to 4-((6bR,10aS)-3-methyl-2,3,6b,9,10,10a-hexahydro-1H-pyrido[3?,4?:4,5]pyrrolo[1,2,3-de]quinoxalin-8(7H)-yl)-1-(4-fluorophenyl)-1-butanone tosylate salt in crystalline and in solid forms, the method of making and using such crystals.
    Type: Grant
    Filed: February 11, 2014
    Date of Patent: December 1, 2015
    Assignee: INTRA-CELLULAR THERAPIES, INC.
    Inventors: John Tomesch, Lawrence P. Wennogle
  • Patent number: 9139836
    Abstract: The present invention provides, among other things, imidazo[1,2-?]pyrazine derivatives according for Formula (Ia) or Formula (Ib). The derivatives are useful in any method which other coelenterazines have been used. For example, the derivatives may be used in a bioluminogenic method to detect the presence of certain compounds or molecules.
    Type: Grant
    Filed: August 18, 2014
    Date of Patent: September 22, 2015
    Assignee: PROMEGA CORPORATION
    Inventors: Dieter H. Klaubert, Poncho Meisenheimer, James Unch
  • Patent number: 9040535
    Abstract: Crystalline molecular complexes of tadalafil are disclosed. The crystalline molecular complexes include those of tadalafil and oxalic acid, tadalafil and 4-hydroxybenzoic acid, tadalafil and 3-phenylpropanoic acid, tadalafil and malonic acid, tadalafil and methylparaben, and tadalafil and propylparaben. Pharmaceutical compositions containing the crystalline molecular complexes are also disclosed.
    Type: Grant
    Filed: October 7, 2013
    Date of Patent: May 26, 2015
    Assignee: THAR PHARMACEUTICALS, INC.
    Inventors: Mazen Hanna, Ning Shan, Miranda L. Cheney, David R. Weyna
  • 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
  • Patent number: 8999522
    Abstract: A 6H-indolo[2,3-b]quinoxaline derivative has a structure of formula (I). R9 is a member selected from the group consisted of an aryl group having one or more substituents and a heteroaryl group having one or more substituents, and R1 to R8 are substituents. The 6H-indolo[2,3-b]quinoxaline derivative of the present invention incorporates an indole and a quinoxaline group therefore inherits good energy transfer ability from indole and good electron-injection ability from quinoxaline. The compound of the present invention may function as a host material or a dopant in the light-emitting layer. In addition, the compound of the present invention may function as hole transport material, electron transport material, hole blocking material, electron blocking material, hole injecting material or electron injecting material.
    Type: Grant
    Filed: September 27, 2010
    Date of Patent: April 7, 2015
    Assignee: National Tsing Hua University
    Inventors: Chien-Hong Cheng, Chun-Hsiang Fan
  • Publication number: 20150079172
    Abstract: The invention relates to particular substituted heterocycle fused gamma-carbolines, their prodrugs, in free, solid, pharmaceutically acceptable salt and/or substantially pure form as described herein, pharmaceutical compositions thereof, and methods of use in the treatment of diseases involving 5-HT2A receptor, serotonin transporter (SERT) and/or pathways involving dopamine D2 receptor signaling systems.
    Type: Application
    Filed: April 14, 2013
    Publication date: March 19, 2015
    Inventors: Sharon Mates, Robert Davis, Peng Li, Lawrence Wennogle, Richard A. Lerner
  • Publication number: 20150080574
    Abstract: A dibenzo[f,h]quinoxaline derivative in which impurities are reduced and a novel method of synthesizing the dibenzo[f,h]quinoxaline derivative in which impurities are reduced are provided. In addition, a light-emitting element, a light-emitting device, an electronic appliance, or a lighting device with high emission efficiency and high reliability in which the dibenzo[f,h]quinoxaline derivative is used as an EL material is provided. In the synthesis method, a 2-(chloroaryl)dibenzo[f,h]quinoxaline derivative is used as a synthetic intermediate in a synthetic pathway so that an impurity contained in a final product can be removed easily by purification by sublimation.
    Type: Application
    Filed: September 12, 2014
    Publication date: March 19, 2015
    Inventors: Hideko Inoue, Tomohiro Kubota, Satoshi Seo, Hayato Yamawaki, Yasushi Kitano
  • Patent number: 8981366
    Abstract: Provided is a heterocyclic compound that can be used for a carrier-transport material, a host material, or a light-emitting material in a light-emitting element. The heterocyclic compound has an indolo[3,2,1-jk]carbazole skeleton and a dibenzo[f,h]quinoxaline skeleton which are linked to each other through an arylene group. The wide band gap of the heterocyclic compound allows excitation of a green-emissive phosphorescent material, which contributes to the formation of a highly efficient light-emitting element.
    Type: Grant
    Filed: May 1, 2014
    Date of Patent: March 17, 2015
    Assignee: Semiconductor Energy Laboratory Co., Ltd.
    Inventors: Hiroshi Kadoma, Yuko Kawata, Hiromi Seo, Tatsuyoshi Takahashi, Satoshi Seo
  • Publication number: 20150073147
    Abstract: A novel organic compound is provided. In addition, a novel organic compound with high heat resistance is provided. In the organic compound, a dibenzoquinoxaline skeleton and a 4,4-bidibenzofuran skeleton or a 4,4?-bidibezothiophene skeleton are connected to each other through an arylene group.
    Type: Application
    Filed: September 11, 2014
    Publication date: March 12, 2015
    Inventors: Hideko INOUE, Hiroki SUZUKI, Hiromi SEO, Tatsuyoshi TAKAHASHI, Satoshi SEO
  • Patent number: 8975403
    Abstract: A simple process for producing v-coelenterazine compounds has been desired. Described is a process for producing a v-coelenterazine compound represented by general formula (II) comprising (1) the step of reacting a compound of general formula (VIII) with a methyltriphenylphosphonium salt in the presence of a base to give a compound represented by general formula (IX), (2) the step of performing a ring-closing metathesis reaction on any one selected from the group consisting of the compound represented by general formula (IX) and a compound of general formula (X) which is the compound of general formula (IX) wherein the amino is protected with R5, and then deprotecting R4 and, if any, R5 to give a v-coelenteramine compound represented by general formula (XIV), and (3) the step of reacting the compound of general formula (XIV) with a compound represented by general formula (XV) to give the compound of general formula (II).
    Type: Grant
    Filed: February 25, 2014
    Date of Patent: March 10, 2015
    Assignees: JNC Corporation, National University Corporation Tokyo Medical and Dental University
    Inventors: Satoshi Inouye, Yuiko Miura, Suguru Yoshida, Takamitsu Hosoya
  • Publication number: 20150064731
    Abstract: The present invention provides, among other things, imidazo[1,2-?]pyrazine derivatives according for Formula (Ia) or Formula (Ib). The derivatives are useful in any method which other coelenterazines have been used. For example, the derivatives may be used in a bioluminogenic method to detect the presence of certain compounds or molecules.
    Type: Application
    Filed: August 18, 2014
    Publication date: March 5, 2015
    Inventors: Dieter H. Klaubert, Poncho Meisenheimer, James Unch
  • Publication number: 20150060818
    Abstract: Provided is a novel organic compound that can be used as a host material of a light-emitting layer in which a light-emitting substance is dispersed. The organic compound is represented by General Formula (G1-1). In the formula, A represents a substituted or unsubstituted dibenzo[f,h]quinoxalin-yl group, Ar1 represents a substituent formed by 1 to 4 rings, and n represents 2 or 3, where the ring is a substituted or unsubstituted benzene ring or a substituted or unsubstituted fluorene ring.
    Type: Application
    Filed: August 27, 2014
    Publication date: March 5, 2015
    Inventors: Yoshimi Ishiguro, Miyako MORIKUBO, Sachiko KAWAKAMI, Hiromi SEO, Tatsuyoshi TAKAHASHI, Satoshi SEO
  • Publication number: 20150060824
    Abstract: Provided is a novel organic compound that is used as a host material in which a light-emitting substance is dispersed. The organic compound is represented by General Formula (G1). In the formula, A represents a substituted or unsubstituted dibenzofuran-diyl group, a substituted or unsubstituted dibenzothiophene-diyl group, a substituted or unsubstituted N-aryl-9H-carbazole-diyl group, or a substituted or unsubstituted N-alkyl-9H-carbazole-diyl group; Ar1 and Ar2 each independently represent a single-bond or a substituted or unsubstituted arylene group; R11 to R19 and R21 to R29 each independently represent hydrogen, an alkyl group having 1 to 6 carbon atoms, or a substituted or unsubstituted aryl group having 6 to 13 carbon atoms; X1 and X2 each independently represent a carbon atom or a nitrogen atom; and the carbon atom is bonded to hydrogen, an alkyl group having 1 to 6 carbon atoms, or a substituted or unsubstituted aryl group having 6 to 13 carbon atoms.
    Type: Application
    Filed: August 29, 2014
    Publication date: March 5, 2015
    Inventors: Yoshimi Ishiguro, Sachiko KAWAKAMI, Hiromi SEO, Tatsuyoshi TAKAHASHI, Satoshi SEO
  • Publication number: 20150060813
    Abstract: A novel heterocyclic compound that can be used as a host material in which a light-emitting substance is dispersed. A light-emitting element having a long lifetime. A heterocyclic compound in which a substituted or unsubstituted dibenzo[f,h]quinoxalinyl group is bonded to a substituted or unsubstituted arylene group having 6 to 25 carbon atoms which is bonded to any one of the 8-11 positions of a substituted or unsubstituted benzo[b]naphtho[1,2-d]furan skeleton.
    Type: Application
    Filed: August 26, 2014
    Publication date: March 5, 2015
    Inventors: Sachiko Kawakami, Hiromi SEO, Tatsuyoshi TAKAHASHI, Satoshi SEO
  • Publication number: 20150048285
    Abstract: Nonlinear optic chromophores comprising stabilized radical structures, mixtures thereof, methods for their production, nonlinear optical materials containing such chromophores, and the use of such materials in electro-optic, solar conversion, photovoltaic and all-optical nonlinear devices are described.
    Type: Application
    Filed: May 21, 2014
    Publication date: February 19, 2015
    Applicant: Lightwave Logic, Inc.
    Inventors: Frederick J. GOETZ, JR., Andrew Ashton, JR., Frederick J. Goetz, SR., David F. Eaton, Anthony J. Arduengo, Howard E. Simmons, III, Jason W. Runyon
  • Publication number: 20150018359
    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 L, R5, W, X, Y1, Y2, and Z 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: July 11, 2014
    Publication date: January 15, 2015
    Inventors: Manoj C. DESAI, Mingzhe JI, Haolun JIN, Teresa Alejandra TREJO MARTIN, Hyung-Jung PYUN
  • Publication number: 20140378432
    Abstract: Heteroaryl pyridone and aza-pyridone compounds are provided, including stereoisomers, tautomers, and pharmaceutically acceptable salts thereof, useful for inhibiting Btk kinase, and for treating immune disorders such as inflammation mediated by Btk kinase. Methods of using heteroaryl pyridone and aza-pyridone compounds for in vitro, in situ, and in vivo diagnosis, and treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed.
    Type: Application
    Filed: September 8, 2014
    Publication date: December 25, 2014
    Inventors: James John Crawford, Daniel Fred Ortwine, BinQing Wei, Wendy B. Young
  • Publication number: 20140364609
    Abstract: The present invention provides methods for the preparation of substituted heterocycle fused gamma-carbolines, intermediates useful in producing them and methods for producing such intermediates and such heterocycle fused gamma-carbolines.
    Type: Application
    Filed: July 3, 2014
    Publication date: December 11, 2014
    Inventors: John Charles TOMESCH, Peng LI, Wei YAO, Qiang ZHANG, James David BEARD, Andrew S. THOMPSON, Hua CHENG, Lawrence P. WENNOGLE
  • Publication number: 20140332758
    Abstract: Donor-acceptor compounds with nitrogen containing polyaromatics as the acceptor with emission originated from the charge transfer (CT) state is disclosed. The donor-acceptor compound is provided that has the structure of Formula 1 shown below: wherein X1 to X12 is independently selected from the group consisting of C—R and N, wherein at least one of X1 to X12 is N, wherein each R is independently selected from the group consisting of hydrogen, deuterium, halide, alkyl, cycloalkyl, heteroalkyl, arylalkyl, alkoxy, aryloxy, amino, silyl, alkenyl, cycloalkenyl, heteroalkenyl, alkynyl, aryl, heteroaryl, acyl, carbonyl, carboxylic acids, ester, nitrile, isonitrile, sulfanyl, sulfinyl, sulfonyl, phosphino, and combinations thereof; and at least one of the R comprises a donor group with at least two electron-donating nitrogens.
    Type: Application
    Filed: May 9, 2013
    Publication date: November 13, 2014
    Applicant: UNIVERSAL DISPLAY CORPORATION
    Inventors: Raymond Kwong, Sui Tung Lam, Chi Hang Lee
  • Publication number: 20140330017
    Abstract: Provided is a heterocyclic compound that can be used for a carrier-transport material, a host material, or a light-emitting material in a light-emitting element. The heterocyclic compound has an indolo[3,2,1-jk]carbazole skeleton and a dibenzo[f,h]quinoxaline skeleton which are linked to each other through an arylene group. The wide band gap of the heterocyclic compound allows excitation of a green-emissive phosphorescent material, which contributes to the formation of a highly efficient light-emitting element.
    Type: Application
    Filed: May 1, 2014
    Publication date: November 6, 2014
    Applicant: Semiconductor Energy Laboratory Co., Ltd.
    Inventors: Hiroshi Kadoma, Yuko Kawata, Hiromi Seo, Tatsuyoshi Takahashi, Satoshi Seo
  • Patent number: 8877351
    Abstract: Disclosed are an organometallic complex emitting red light with high color purity. An organometallic complex having a structure represented by the following general formula (G1) is provided. In the formula, of R1 to R13, at least one represents an alkyl group having 1 to 4 carbon atoms or an alkoxy group having 1 to 4 carbon atoms and the other or others represent hydrogen. M represents a central metal, which is a Group 9 or Group 10 element. L represents a monoanionic ligand, and n is 2 when the central metal is a Group 9 element or 1 when the central metal is a Group 10 element.
    Type: Grant
    Filed: June 23, 2009
    Date of Patent: November 4, 2014
    Assignee: Semiconductor Energy Laboratory Co., Ltd.
    Inventors: Hideko Inoue, Satoshi Seo
  • Publication number: 20140323491
    Abstract: The present invention relates to toluenesulfonic acid addition salt crystals of specific substituted heterocycle fused gamma-carbolines, the method of making and using such crystals.
    Type: Application
    Filed: February 11, 2014
    Publication date: October 30, 2014
    Applicant: INTRA-CELLULAR THERAPIES, INC.
    Inventors: John Tomesch, Lawrence P. Wennogle
  • Patent number: 8871932
    Abstract: The present invention relates to a process for the preparation of tadalafil of Formula I, comprising reacting a D-tryptophan compound of Formula III with piperonal in sulfolane.
    Type: Grant
    Filed: April 10, 2013
    Date of Patent: October 28, 2014
    Assignee: Ranbaxy Laboratories Limited
    Inventors: Dattatray Bapuso Patil, Killol Patel, Ashok Prasad, Mohan Prasad
  • Publication number: 20140271847
    Abstract: There is disclosed a formulation for creating a rapid penile erection within 30 minutes. In an embodiment, a lozenge has a preparation configured to create a rapid penile erection. The preparation is effective to create the rapid penile erection with sildenafil citrate in a range of 50-100 mg. The preparation is effective to create the rapid penile erection with tadalafil in a range of 5-40 mg. The preparation is effective to create the rapid penile erection with vardenafil hydrochloride in a range of 5-40 mg. In various embodiments, the formulation includes a solvent configured to permeate skin. Other embodiments are also disclosed.
    Type: Application
    Filed: March 13, 2014
    Publication date: September 18, 2014
    Inventors: Ray L. Hauser, BoLin Zheng
  • Publication number: 20140275530
    Abstract: The present invention describes triphenylene derivatives, in particular for use as triplet matrix materials in organic electroluminescent devices. The invention furthermore relates to a process for the preparation of the compounds according to the invention and to electronic devices comprising same.
    Type: Application
    Filed: September 24, 2012
    Publication date: September 18, 2014
    Inventors: Anja Jatsch, Rémi Manouk Anémian, Bernd Schroeder, Arne Buesing, Philipp Stoessel, Christof Pflumm, Jonas Valentin Kroeber, Thomas Eberle
  • Publication number: 20140256937
    Abstract: The present invention relates to a novel compound having an antiviral effect, more specifically, a pyridone derivative having HIV integrase inhibitory activity, and a medicament containing the same, in particular, an anti-HIV agent. The compound of the present invention has integrase inhibitory activity and/or cell proliferation inhibitory activity against viruses, in particular, HIV and drug-resistant strains thereof. Thus, the compound is useful in preventing or treating various diseases, viral infections (for example, AIDS), and the like in which integrase participates.
    Type: Application
    Filed: October 12, 2012
    Publication date: September 11, 2014
    Applicant: SHIONOGI & CO., LTD.
    Inventor: Toshiyuki Akiyama
  • Publication number: 20140235644
    Abstract: The disclosure describes compounds of formula I, wherein the wedged bonds, R1, R2, R3, R4, R5, R5a, R6, R7, R8, R9, R10, R11, R12, R13, R14, X and Y have meanings given in the description, and pharmaceutically-acceptable salts thereof; and methods of using such compounds useful in the treatment of cancer and conditions affected by inhibition of angiogenesis. Also provided, are processes for the preparation of formula I, by reacting formula I with other compounds; and processes for the preparation of a pharmaceutical formulation by bringing into association, a compound of formula I, with therapeutic agents and/or a pharmaceutically-acceptable adjuvant, diluent, or carrier.
    Type: Application
    Filed: April 28, 2014
    Publication date: August 21, 2014
    Applicant: Everest Biosciences, Inc.
    Inventors: Jenny Persson, Rikard Larsson, Olov Sterner, Martin Johansson
  • 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: 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: 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: 20140206868
    Abstract: A simple process for producing v-coelenterazine compounds has been desired. Described is a process for producing a v-coelenterazine compound represented by general formula (II) comprising (1) the step of reacting a compound of general formula (VIII) with a methyltriphenylphosphonium salt in the presence of a base to give a compound represented by general formula (IX), (2) the step of performing a ring-closing metathesis reaction on any one selected from the group consisting of the compound represented by general formula (IX) and a compound of general formula (X) which is the compound of general formula (IX) wherein the amino is protected with R5, and then deprotecting R4 and, if any, R5 to give a v-coelenteramine compound represented by general formula (XIV), and (3) the step of reacting the compound of general formula (XIV) with a compound represented by general formula (XV) to give the compound of general formula (II).
    Type: Application
    Filed: February 25, 2014
    Publication date: July 24, 2014
    Applicants: NATIONAL UNIVERSITY CORPORATION TOKYO MEDICAL AND DENTAL UNIVERSITY, JNC CORPORATION
    Inventors: Satoshi INOUYE, Yuiko MIURA, Suguru YOSHIDA, Takamitsu HOSOYA
  • Publication number: 20140200209
    Abstract: The present invention is to provide a novel compound (I) shown below, having the anti-virus activity; particularly the HIV integrase inhibitory activity, and a drug containing the same, particularly an anti-HIV drug, as well as a process and an intermediate thereof. (wherein Z1 is NR4; R1 is hydrogen or lower alkyl; X is a single bond, a hetero atom group selected from O, S, SO, SO2 and NH, or lower alkylene or lower alkenylene in which the hetero atom group may intervene; R2 is optionally substituted aryl; R3 is hydrogen, a halogen, hydroxy, optionally substituted lower alkyl etc; and R4 and Z2 part taken together forms a ring, to form a polycyclic compound, including e.g., a tricyclic or tetracyclic compound.
    Type: Application
    Filed: March 14, 2014
    Publication date: July 17, 2014
    Applicants: ViiV Healthcare Company, Shionogi & Co., Ltd.
    Inventors: Brian A. JOHNS, Takashi KAWASUJI, Teruhiko TAISHI, Yoshiyuki TAODA
  • Publication number: 20140200219
    Abstract: The present methods and compositions are of use for treatment of conditions involving fibrosis, such as Peyronie's disease plaque, penile corporal fibrosis, penile veno-occlusive dysfunction, Dupuytren's disease nodules, vaginal fibrosis, clitoral fibrosis, female sexual arousal disorder, abnormal wound healing, keloid formation, general fibrosis of the kidney, bladder, prostate, skin, liver, lung, heart, intestines or any other localized or generalized fibrotic condition, vascular fibrosis, arterial intima hyperplasia, atherosclerosis, arteriosclerosis, restenosis, cardiac hypertrophy, hypertension or any condition characterized by excessive fibroblast or smooth muscle cell proliferation or deposition of collagen and extracellular matrix in the blood vessels and/or heart.
    Type: Application
    Filed: March 17, 2014
    Publication date: July 17, 2014
    Applicant: Los Angeles Biomedical Research Institute at Harbor-UCLA Medical Center
    Inventors: Nestor F. Gonzalez-Cadavid, Jacob Rajfer
  • Patent number: 8778943
    Abstract: The present invention is directed to a class of substituted 10-hydroxy-9,11-dioxo-2,3,4a,5,9,11,13,13a-octahydro-1H-pyrido[1,2-a]pyrrolo[1?,2?:3,4]imidazo[1,2-d]pyrazine-8-carboxamides useful as anti-HIV agents. The compounds have the formula (I-1-1): wherein ring A is an optionally substituted hexahydro-1H-pyrrolo[1,2-c]-imidazole; R14 and RX are independently hydrogen or optionally substituted lower alkyl; R3 is selected from various groups; R1 is hydrogen or lower alkyl; R is halogen; m is 0, 1, 2 or 3; or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: February 8, 2013
    Date of Patent: July 15, 2014
    Assignees: Shionogi & Co., Ltd., ViiV Healthcare Company
    Inventors: Brian A. Johns, Takashi Kawasuji, Teruhiko Taishi, Yoshiyuki Taoda
  • Publication number: 20140187500
    Abstract: The present application provides, among other things, compounds, compositions and methods for treating various diseases including cancer.
    Type: Application
    Filed: December 4, 2013
    Publication date: July 3, 2014
    Applicants: The Board of Trustees of the University of Illinois, Massachusetts Institute of Technology
    Inventors: Mohammad Movassaghi, Justin Kim, Paul J. Hergenrother
  • Publication number: 20140179669
    Abstract: The present invention relates to compounds defined by formula I wherein the groups A, B, X, m, n and o 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: February 27, 2014
    Publication date: June 26, 2014
    Applicant: Boehringer Ingelheim International GmbH
    Inventors: Stefan PETERS, Matthias ECKHARDT, Bradford S. HAMILTON, Frank HIMMELSBACH, Joerg KLEY
  • Patent number: 8754214
    Abstract: A synthesis approach providing an early ring attachment via a bromination to compound I-I yielding compound II-II: whereby a final product such as AA: can be synthesized. In particular, the 2,4-difluorophenyl-containing sidechain is attached before creation of the additional ring Q.
    Type: Grant
    Filed: December 4, 2013
    Date of Patent: June 17, 2014
    Assignees: Shionogi & Co., Ltd., ViiV Healthcare Company
    Inventors: Hiroshi Yoshida, Yoshiyuki Taoda, Brian Alvin Johns, Takashi Kawasuji, Daiki Nagamatsu
  • Publication number: 20140142309
    Abstract: The present invention relates to a process for the preparation of a cis-intermediate compound of Formula II which is a useful synthetic intermediate for the preparation of tadalafil of Formula I—a potent, selective, and reversible inhibitor of cyclic guanosine 3?,5?-monophosphate specific phosphodiesterase type 5 enzyme having phosphodiesterase inhibitory activity.
    Type: Application
    Filed: April 10, 2013
    Publication date: May 22, 2014
    Applicant: RANBAXY LABORATORIES LIMITED
    Inventors: Dattatray B. PATIL, Killol Patel, Ashok Prasad, Mohan Prasad
  • Publication number: 20140128606
    Abstract: An antipruritic which exerts an antipruritic effect based on a novel action mechanism and is effective for pruritus. The antipruritic contains as an effective ingredient a compound which activates a central type nicotinic acetylcholine receptor.
    Type: Application
    Filed: June 29, 2012
    Publication date: May 8, 2014
    Applicant: Toray Industries, Inc.
    Inventor: Kenichi Hayashi
  • Publication number: 20140124764
    Abstract: To provide a novel heterocyclic compound capable of being used as a host material in which a light-emitting substance is dispersed. To provide a light-emitting element having a long lifetime. A heterocyclic compound in which a dibenzo[f,h]quinoxalinyl group and a benzo[b]naphtho[1,2-d]furanyl group are bonded through an arylene group having 6 to 13 carbon atoms. The dibenzo[f,h]quinoxalinyl group, the benzo[b]naphtho[1,2-d]furanyl group, and the arylene group separately are unsubstituted or have, as a substituent, an alkyl group having 1 to 4 carbon atoms or an aryl group having 6 to 13 carbon atoms.
    Type: Application
    Filed: October 31, 2013
    Publication date: May 8, 2014
    Applicant: Semiconductor Energy Laboratory Co., Ltd.
    Inventors: Yasushi Kitano, Hiroshi Kadoma, Satoko Shitagaki, Satoshi Seo, Hiromi Seo, Tatsuyoshi Takahashi