Two Ring Nitrogens In The Tetracyclo Ring System Patents (Class 546/70)
  • Patent number: 10011598
    Abstract: The invention provides a series of bioactive small molecules that target expanded r(CGG) repeats, termed r(CGG)exp, that causes Fragile X-associated Tremor Ataxia Syndrome (FXTAS). The compound was identified by using information on the chemotypes and RNA motifs that interact. Specifically, 9-hydroxy-5,11-dimethyl-2-(2-(piperidin-1-yl)ethyl)-6H-pyrido[4,3-b]carbazol-2-ium, binds the 5?CGG/3?GGC motifs in r(CGG)exp and disrupts a toxic r(CGG)exp-protein complex. Specifically, dimeric compounds incorporating two 9-hydroxyellipticine analog structures can even more potently bind the 5?CGG/3?GGC motifs in r(CGG)exp and disrupts a toxic r(CGG)exp-protein complex. Structure-activity relationships (SAR) studies determined that the alkylated pyridyl and phenolic side chains are important chemotypes that drive molecular recognition of r(CGG) repeats, such as r(CGG)exp.
    Type: Grant
    Filed: January 23, 2017
    Date of Patent: July 3, 2018
    Assignee: The Scripps Research Institute
    Inventors: Matthew D. Disney, Biao Liu, Jessica L. Childs-Disney, Wang-Yong Yang
  • Patent number: 9073920
    Abstract: The invention described herein pertains to substituted dibenzonaphthyridine compounds, pharmaceutical compositions, and formulations comprising the dibenzonaphthyridine compounds, their synthesis, and methods for their use in the treatment and/or prevention of cancer.
    Type: Grant
    Filed: August 17, 2011
    Date of Patent: July 7, 2015
    Assignee: Purdue Research Foundation
    Inventors: Mark S. Cushman, Evgeny A. Kiselev
  • Publication number: 20150141419
    Abstract: The present invention relates to a diarylo[a,g]quinolizidine compound of formula (I), enantiomer, diastereoisomer, racemate, mixture, pharmaceutically acceptable salt, crystalline hydrate or solvate thereof; the preparation method thereof, and uses thereof in preparing an experimental model drugs related to dopamine receptors and 5-HT receptors or a medicament for treating or preventing a disease related to dopamine receptors and 5-HT receptors.
    Type: Application
    Filed: May 9, 2013
    Publication date: May 21, 2015
    Inventors: Hong Liu, Xuechu Zhen, Haifeng Sun, Liyuan Zhu, Wangke Qian, Leiping Yu, Zeng Li, Shengbin Zhou, Wenxian Cai, Hualiang Jiang, Kaixian Chen
  • Patent number: 9034870
    Abstract: The invention described herein pertains to substituted azaindenoisoquinoline compounds, in particular 7-, 8-, 9-, and 10-azaindenoisoquinoline compounds, which are inhibitors of topoisomerase I, processes and intermediates for their syntheses, pharmaceutical compositions of the compounds, and methods of using them in the treatment of cancer.
    Type: Grant
    Filed: March 6, 2014
    Date of Patent: May 19, 2015
    Assignees: Purdue Research Foundation, United States Government National Institutes of Health (NIH), U.S. Dept. of Health and Human Services (DHHS), NIH Division of Extramural Inventions and Technology Resources (DEITR)
    Inventors: Mark S. Cushman, Evgeny A. Kiselev, Andrew E. Morrell, Yves George Pommier
  • Publication number: 20150051194
    Abstract: 8-Substituted-2,6-methano-3-benzazocines of general structure are useful as analgesics, anti-diarrheal agents, anticonvulsants, antitussives and anti-addiction medications.
    Type: Application
    Filed: October 31, 2014
    Publication date: February 19, 2015
    Applicant: RENSSELAER POLYTECHNIC INSTITUTE
    Inventor: Mark P. WENTLAND
  • Publication number: 20150038438
    Abstract: The present description relates to compounds and forms and pharmaceutical compositions thereof and methods for use thereof to treat or ameliorate bacterial infections caused by wild-type and multi-drug resistant Gram-negative and Gram-positive pathogens.
    Type: Application
    Filed: August 29, 2012
    Publication date: February 5, 2015
    Inventors: Arthur Branstrom, Vara Prasad Venkata Nagendra Josyula, Michael Andrew Arnold, Aleksey I. Gerasyuto, Gary Karp, Jiashi Wang, Guangming Chen, Olya Ginzburg, Song Huang, Jana Narasimhan, Srinivasa Peddi, Sean Wesley Smith, Anthony Allan Turpoff, Matthew G. Woll, Nanjing Zhang, Xiaoyan Zhang
  • Publication number: 20150018380
    Abstract: The present invention provides methods for obtaining specific and non-toxic inhibitors of AID nuclear import. The methods comprise a primary screen and a counter screen to identify a pool of AID specific nuclear import inhibitors that do not have off-target of toxic effects. AID specific nuclear import inhibitors identified by the screens of the invention prevent nuclear entry, limit the access of AID to genomic DNA, and inhibit AID mutagenic activity. Preparations, including pharmaceutical preparations, comprising specific nuclear import inhibitors, used for example, to inhibit cancer progression, are also encompassed in the invention.
    Type: Application
    Filed: February 7, 2013
    Publication date: January 15, 2015
    Applicant: University of Rochester
    Inventor: Harold C. Smith
  • Publication number: 20150010461
    Abstract: Provided are methods for preparing and using reaction vessels obtained or obtainable by 3D-printin methods, including a method for preparing a product compound, the method comprising the steps of: (i) providing a reaction vessel that is obtained by a 3-D printing method, wherein the reaction vessel has a reaction space; (ii) providing one or more reagents, optionally together with a catalyst or a solvent, for use in the synthesis of the product compound; and (iii) permitting the one or more reagents to react in the reaction space, optionally in the presence of the catalyst and the solvent, in the reaction vessel, thereby to form the product compound.
    Type: Application
    Filed: February 18, 2013
    Publication date: January 8, 2015
    Inventor: Leroy Cronin
  • Publication number: 20140374733
    Abstract: An object of the present invention is to provide a photoelectric conversion element having a photoelectric conversion film which exhibits heat resistance, a high photoelectric conversion efficiency, a low level of dark currents, rapid response, and sensitivity characteristics to red and can be produced by a vapor deposition processing that is continuously performed under a high-temperature condition. The photoelectric conversion element of the present invention is a photoelectric conversion element in which a conductive film, a photoelectric conversion film containing a photoelectric conversion material, and a transparent conductive film are laminated on one another in this order, wherein the photoelectric conversion material includes a compound represented by Formula (1).
    Type: Application
    Filed: September 5, 2014
    Publication date: December 25, 2014
    Applicant: FUJIFILM Corporation
    Inventors: Yuki HIRAI, Yosuke YAMAMOTO, Tomoaki YOSHIOKA, Eiji FUKUZAKI, Katsuyuki YOFU, Masaaki TSUKASE, Mitsumasa HAMANO, Takahiko ICHIKI
  • Publication number: 20140364443
    Abstract: Disclosed are 1,4-dihydro-naphthyridine derivatives and pharmaceutical composition and uses thereof. The 1,4-dihydro-naphthyridine derivatives are a compound capable of inhibiting acetylcholinesterase activity and preventing extracellular calcium from flowing into a cell via a calcium channel, i.e., having a dual-activity, which are of potential importance as a pharmaceutical and can be used to prepare the drugs for treating cardiovascular diseases, cerebrovascular diseases and dementia.
    Type: Application
    Filed: December 7, 2012
    Publication date: December 11, 2014
    Applicant: Jiangsu Simovay Pharmaceutical Co., Ltd.
    Inventors: Rong Chen, Lin Feng, Zhengping Zhang, Fang Fang, Qingli Dong, Fulong Li, Lei Wang, Yao Hua, Shibao Yang, Peng Wang
  • 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
  • Patent number: 8877354
    Abstract: An organic light-emitting device includes an anode, a cathode, and an organic compound layer interposed between the anode and the cathode. The organic compound layer contains a heterocyclic compound represented by general formula [1]: (wherein R1 and R2 each independently represent a hydrogen atom, a substituted or unsubstituted alkyl group, a substituted or unsubstituted aryl group having three or less rings, or a substituted or unsubstituted heterocyclic group having three or less rings; R1 and R2 may be the same as or different from each other; R3 and R4 each independently represent a hydrogen atom, a substituted or unsubstituted aryl group having three or less rings, or a substituted or unsubstituted heterocyclic group having three or less rings; one of R3 and R4 represents a substituted or unsubstituted aryl group having three or less rings or a substituted or unsubstituted heterocyclic group having three or less rings; and R3 and R4 may be the same as or different from each other).
    Type: Grant
    Filed: August 5, 2010
    Date of Patent: November 4, 2014
    Assignee: Canon Kabushiki Kaisha
    Inventors: Takayuki Horiuchi, Jun Kamatani, Akihito Saitoh
  • Publication number: 20140322636
    Abstract: An electrophotographic photosensitive member includes a support, an undercoat layer formed on the support, and a photosensitive layer formed on the undercoat layer, in which the undercoat layer contains a polymerized product of a compound represented by the formula (1) or a polymerized product of a composition containing a compound represented by the formula (1).
    Type: Application
    Filed: April 23, 2014
    Publication date: October 30, 2014
    Applicant: CANON KABUSHIKI KAISHA
    Inventors: Kunihiko Sekido, Nobuhiro Nakamura, Atsushi Okuda, Michiyo Sekiya, Yota Ito
  • Publication number: 20140309182
    Abstract: The present invention relates to an insecticidal enriched extract (biopesticide) isolated from the stem of Nothapodites foetida (Wight) Sleumer (formerly Mappia foetida (Miers) useful for the insect free storage and transport of grains and seed. The insecticidal activity of the enriched extract (biopesticide) of the invention is ascribed to compound/s other than camptothecin. The invention further relates to the process for preparation thereof, containing Compounds of general formula 1 and formula 2 (General formula 1) wherein R1=CH3, CH2OAC and wherein R2=COOH, or (I) and R3=H. OH.
    Type: Application
    Filed: June 21, 2012
    Publication date: October 16, 2014
    Inventors: Swati Pramod Joshi, John Pereira, Phool Kumar Patanjali, Sunita Sharad Kunte, Kiran Babasaheb Sonawane, Suresh Gurappa Mummigatti, Sumithra Devi Sanna, Krishnaiah Eraiah Hullukere, Seema Chaudhary
  • 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
  • Publication number: 20140296209
    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 ?1B—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 2, 2014
    Applicant: MEDIVATION TECHNOLOGIES, INC.
    Inventors: Andrew Asher Protter, Sarvajit Chakravarty
  • Patent number: 8822688
    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: Grant
    Filed: October 26, 2012
    Date of Patent: September 2, 2014
    Assignee: Astellas Pharma Inc.
    Inventors: Kiyohiro Samizu, Naoyuki Masuda, Kazuhiko Iikubo, Yohei Koganemaru, Noriyuki Kawano, Junya Ohmori, Yasuyuki Mitani, Keni Ni
  • Patent number: 8808877
    Abstract: A method of manufacturing an organic EL element, which may be a top-emitting or a transparent organic EL element, provides an organic EL element having a low driving voltage and a high efficiency. The organic EL element includes a substrate; an anode; an organic EL layer which includes at least an emissive layer, an electron transport layer and a damage-mitigating electron injection layer; and a transparent cathode composed of a transparent conductive oxide material, the damage-mitigating electron injection layer is in contact with the transparent cathode, and the damage-mitigating electron injection layer includes a crystalline oligothiophene compound.
    Type: Grant
    Filed: August 18, 2009
    Date of Patent: August 19, 2014
    Assignee: Sharp Kabushiki Kaisha
    Inventor: Yutaka Terao
  • 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: 20140187547
    Abstract: The invention described herein pertains to substituted azaindenoisoquinoline compounds, in particular 7-, 8-, 9-, and 10-azaindenoisoquinoline compounds, which are inhibitors of topoisomerase I, processes and intermediates for their syntheses, pharmaceutical compositions of the compounds, and methods of using them in the treatment of cancer.
    Type: Application
    Filed: March 6, 2014
    Publication date: July 3, 2014
    Applicant: Purdue Research Foundation
    Inventors: Mark S. CUSHMAN, Evgeny A. KISELEV, Andrew E. MORRELL
  • 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
  • Publication number: 20140151650
    Abstract: A heterocyclic compound represented by Formula 1 below and an organic light-emitting device including the heterocyclic compound are described. In Formula 1, R1 to R4 may be each independently one of a hydrogen atom, a deuterium atom, C5-C60 alkyl, C5-C60 aryl and C6-C60 condensed polycyclic; L1 and L2 may be each independently one of a single bond, C5-C60 aryl, C3-C60 heteroaryl and C6-C60 condensed polycyclic; Ar1 and Ar2 may be each independently one of C5-C60 aryl, C3-C60 heteroaryl and C6-C60 condensed polycyclic; A, B, C and D may be each independently one of —CH? and —N?, excluding that all A, B, C and D are —CH?; and m and n may be each independently an integer of 0 to 3, excluding that all m and n are zero, wherein any of the above alkyl groups, aryl groups, condensed polycyclic groups and heteroaryl groups may be substituted or unsubstituted.
    Type: Application
    Filed: August 28, 2013
    Publication date: June 5, 2014
    Inventor: Jung-Sub Lee
  • Patent number: 8703951
    Abstract: The present invention provides a series of 2,3-bis(hydroxymethyl)-4H-benzo[d]pyrrolo-[1,2-a]thiazoles and 1,2-bis(hydroxymethyl)indolizino[6,7-b]indole derivatives and their bis(alkylcarbamates) derivatives. These derivatives were designed as bi-functional DNA cross-linking agents. The in vitro cytotoxicity study of these compounds revealed that they exhibit significant anti-proliferative activity in inhibiting human lymphoblastic leukemia and various solid tumor cell growth. The compounds also exhibit therapeutic efficacy against human breast carcinoma and lung cancer in xenograft model. The compounds generally possess potent antitumor activity to kill various human solid tumors and have high potential for clinical applications.
    Type: Grant
    Filed: July 16, 2012
    Date of Patent: April 22, 2014
    Assignee: Academia Sinica
    Inventors: Tsann-Long Su, Ting-Chao Chou, Te-Chang Lee
  • Patent number: 8686144
    Abstract: The invention relates to the use of specific compounds of formula (I) and their pharmaceutically-acceptable salts: (Formula 1) (I) as a new family of protein kinase CK2 inhibitors; the invention also relates to the use of compounds of formula (I) for the preparation of pharmaceutical compositions for the prevention and/or treatment of disorders and/or diseases chosen amongst cancers; autoimmune and inflammatory diseases; infectious diseases; diabetes angiogenesis related disorders; retinopathies and cardiac hypertrophy.
    Type: Grant
    Filed: July 28, 2010
    Date of Patent: April 1, 2014
    Assignees: Commissariat a l'Energie Atomique et aux Energie Alternative, Institut National de la Sante et de la Recherche Medicale (INSERM), Institut Curie, Centre National de la Recherche Scientifique
    Inventors: Claude Cochet, Renaud Prudent, Virginie Moucadel, Chi-Hung N'guyen
  • Publication number: 20140088305
    Abstract: The present invention relates to organic electroluminescent devices which comprise heteroaromatic compounds.
    Type: Application
    Filed: May 7, 2012
    Publication date: March 27, 2014
    Applicant: Merck Patent GmbH
    Inventors: Amir Hossain Parham, Arne Buesing, Christof Pflumm, Teresa Mujica-Fernaud, Philipp Toessel, Thomas Eberle
  • Publication number: 20140073637
    Abstract: The present invention relates to a new class of benzo[e]pyrido-indole, the amino-substituted-alkyloxy-benzo[e]pyrido[4,3-b]indole derivatives, having a particular kinase inhibition profile and useful as a therapeutic agent, in particular an anti-tumoral agent.
    Type: Application
    Filed: May 30, 2012
    Publication date: March 13, 2014
    Applicants: INSTITUT CURIE, INSERM (INSTITUT NATIONAL DE LA SANTE ET DE LA RECHERCHE MEDICALE, CENTRE NATIONAL DE LA RECHERCHE SCIENTIFIQUE
    Inventors: Chi-Hung N'Guyen, Annie Molla, Ly-Thuy-Tram Le
  • 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: 20140042370
    Abstract: The present invention relates to compounds of the formula (1) and formula (2), which are suitable for use in electronic devices, in particular in organic electroluminescent devices.
    Type: Application
    Filed: March 26, 2012
    Publication date: February 13, 2014
    Applicant: MERCK PATENT GMBH
    Inventors: Irina Martynova, Christof Pflumm, Amir Hossain Parham, Christof Pflumm, Rémi Manouk Anémian, Teresa Mujica-Fernaud, Claire De Nonancourt
  • Patent number: 8642610
    Abstract: The present invention provides analogs and derivatives of thalidomide which inhibit cancer and angiogenesis. The present invention further provides compounds which disrupt microtubule polymerization. The present further provides methods of treating cancers comprising mutant p53.
    Type: Grant
    Filed: February 6, 2012
    Date of Patent: February 4, 2014
    Assignee: University of Virginia Patent Foundation
    Inventor: Milton L. Brown
  • Publication number: 20140027755
    Abstract: The present invention relates to an electronic device comprising one or more compounds of a formula (I) or (II). Furthermore, the invention encompasses the use of a compound of the formula (I) or (II) in an electronic device, and the provision of certain compounds of the formula (I) or (II).
    Type: Application
    Filed: March 15, 2012
    Publication date: January 30, 2014
    Applicant: Merck Patent GmbH Patents & Scientific Information
    Inventors: Teresa Mujica-Fernaud, Christof Pflumm, Irina Martynova
  • Publication number: 20140014930
    Abstract: A novel organic compound with which the emission characteristics, emission efficiency, and reliability of a light-emitting element can be improved is provided. The organic compound has an imidazo[1,2-f]phenanthridine skeleton and a dibenzothiophene skeleton or a dibenzofuran skeleton bonded through an arylene group. The light-emitting element including the organic compound in a light-emitting layer shows high efficiency and low power consumption.
    Type: Application
    Filed: July 11, 2013
    Publication date: January 16, 2014
    Applicant: Semiconductor Energy Laboratory Co., Ltd.
    Inventors: Tomoya Hirose, Hiroshi Kadoma, Satoko Shitagaki, Satoshi Seo
  • Publication number: 20140018360
    Abstract: The invention described herein pertains to substituted azaindenoisoquinoline compounds, in particular 7-, 8-, 9-, and 10-azaindenoisoquinoline compounds, which are inhibitors of topoisomerase I, processes and intermediates for their syntheses, pharmaceutical compositions of the compounds, and methods of using them in the treatment of cancer.
    Type: Application
    Filed: July 13, 2012
    Publication date: January 16, 2014
    Inventors: Mark S. CUSHMAN, Evgeny A. KISELEV, Andrew E. MORRELL
  • Patent number: 8618299
    Abstract: MCH-1 receptor antagonists are disclosed having the general formula These compounds are used in the treatment of various disorders, including obesity, anxiety, depression, non-alcoholic fatty liver disease, and psychiatric disorders. Methods of making these compounds are also described in the present invention.
    Type: Grant
    Filed: July 1, 2010
    Date of Patent: December 31, 2013
    Assignee: Albany Molecular Research, Inc.
    Inventors: Peter R. Guzzo, Matthew David Surman, Alan John Henderson, May Xiaowu Jiang
  • Patent number: 8604048
    Abstract: Pyridocarbazole-type compounds of formula (I): are provided as a medicament, and more particularly for application in anticancer chemotherapy. Also provided is a pharmaceutical composition with the compound and methods for preventing and/or treating neurodegenerative-type pathologies, such as Alzheimer's disease and schizophrenia, parasitoses, such as malaria, or glaucomas.
    Type: Grant
    Filed: February 19, 2010
    Date of Patent: December 10, 2013
    Assignees: Centre National de la Recherche Scientifique, Institut Curie, Commissariat a l'Energie Atomique et aux Energies Alternatives, Universite Paris Sud (Paris XI)
    Inventors: Laurence Lafanechere, Emilie Vassal, Caroline Barette, ChiHung Nguyen, Christian Rivalle, Renaud Prudent
  • Publication number: 20130240866
    Abstract: There is provided a compound having Formula I or Formula II where: Ar1—Ar4 are the same or different and are H, D, or aryl.
    Type: Application
    Filed: December 12, 2011
    Publication date: September 19, 2013
    Applicant: E I DU PONT DE NEMOURS AND COMPANY
    Inventors: Kalindi Dogra, Adam Fennimore, Christina M. Older, Robert A. Eakin
  • 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: 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: 20130190293
    Abstract: This disclosure is directed to tetracyclic pyrido[4,3-b]indole and pyrido[3,4-b]indoles. 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 25, 2013
    Inventors: Sarvajit Chakravarty, Barry Patrick Hart, Rajendra Parasmal Jain
  • Publication number: 20130190308
    Abstract: This disclosure relates to new heterocyclic compounds that may be used to modulate a histamine receptor in an individual. Pyrido[3,4-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: 20130187136
    Abstract: Acenes, such as aza-acenes are attractive materials for organic semiconductors, specifically for n-type materials. There are disclosed new derivatives of acenes that are fabricated using novel synthesis. For example, the disclosed fabrication strategies have allowed for the first time new aza-tetracene and aza-pentacene derivatives. The HOMO and LUMO energy levels of these materials are tunable through appropriate substitution and as predicted, deepened. There are also disclosed organic photosensitive devices comprising at least one aza-acene such as aza-tetracene and aza-pentacene.
    Type: Application
    Filed: January 22, 2013
    Publication date: July 25, 2013
    Applicant: University of Southern California
    Inventors: Mark E. Thompson, Jonathan R. Sommer, Andrew Bartynski
  • 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: 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: 20130178629
    Abstract: The present invention provides a series of 2,3-bis(hydroxymethyl)-4H-benzo[d]pyrrolo-[1,2-a]thiazoles and 1,2-bis(hydroxymethyl)indolizino[6,7-b]indole derivatives and their bis(alkylcarbamates) derivatives. These derivatives were designed as bi-functional DNA cross-linking agents. The in vitro cytotoxicity study of these compounds revealed that they exhibit significant anti-proliferative activity in inhibiting human lymphoblastic leukemia and various solid tumor cell growth. The compounds also exhibit therapeutic efficacy against human breast carcinoma and lung cancer in xenograft model. The compounds generally possess potent antitumor activity to kill various human solid tumors and have high potential for clinical applications.
    Type: Application
    Filed: July 16, 2012
    Publication date: July 11, 2013
    Applicant: Academia Sinica
    Inventors: Tsann-Long Su, Ting-Chao Chou, Te-Chang Lee
  • 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: 20130158063
    Abstract: Disclosed are compounds, compositions and methods related PPAR antagonists. Certain compounds are effective at inhibiting PPARs. The compositions can be used to inhibit PPARs, treat cancer and treat metabolic disorders.
    Type: Application
    Filed: August 24, 2011
    Publication date: June 20, 2013
    Applicant: GEORGETOWN UNIVERSITY
    Inventors: Milton Lang Brown, Yali Kong, Yong Liu, Robert Glazer, York Tomita
  • Publication number: 20130143878
    Abstract: The invention described herein pertains to substituted dibenzonaphthyridine compounds, pharmaceutical compositions, and formulations comprising the dibenzonaphthyridine compounds, their synthesis, and methods for their use in the treatment and/or prevention of cancer.
    Type: Application
    Filed: August 17, 2011
    Publication date: June 6, 2013
    Applicant: PURDUE RESEARCH FOUNDATION
    Inventors: Mark S. Cushman, Evgeny A. Kiselev
  • Patent number: 8431564
    Abstract: The invention relates to ring-annulated dihydropyrrolo[2,1-a]isoquinoline compounds according to general Formula I or a pharmaceutically acceptable salt thereof. The compounds can be used for the treatment of infertility.
    Type: Grant
    Filed: July 27, 2010
    Date of Patent: April 30, 2013
    Assignee: Merck Sharp & Dohme B.V.
    Inventors: Cornelis Marius Timmers, Hubert Jan Jozef Loozen, Herman Thijs Stock
  • Publication number: 20130099206
    Abstract: A heterocyclic compound represented by Formula 1 below, and an organic light-emitting diode including the heterocyclic compound, and a flat display device including the organic light-emitting diode. wherein Ar1 to Ar4, X1, X2, Y1, Y2, L1, and m are defined as in the specification.
    Type: Application
    Filed: March 7, 2012
    Publication date: April 25, 2013
    Applicant: SAMSUNG MOBILE DISPLAY CO., LTD.
    Inventors: Hye-Jin Jung, Seok-Hwan Hwang, Young-Kook Kim, Jin-O Lim, Sang-Hyun Han, Jong-Hyuk 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.