The Six-membered Hetero Ring Shares Ring Members With The Five-membered Cyclo Only (e.g., Pyrido-indoles, Etc.) Patents (Class 546/85)
  • Patent number: 10647724
    Abstract: The present disclosure provides compounds of Formula (I) and Formula (II). The compounds described herein may be useful in treating proliferative diseases (e.g., cancer). Also provided in the present disclosure are pharmaceutical compositions, kits, methods, and uses including or using a compound described herein.
    Type: Grant
    Filed: February 3, 2017
    Date of Patent: May 12, 2020
    Assignee: INVENTISBIO INC.
    Inventors: Xing Dai, Yaolin Wang
  • Patent number: 10398678
    Abstract: Provided are compositions for inhibiting a biological activity of an aldo-keto reductase family 1, member C3 (AKR1C3) polypeptide. In some embodiments, the compositions are indomethacin derivatives that are AKR1C3-specific inhibitors. Also provided are methods for producing disclosed indomethacin derivatives that substantially lack cyclooxygenase inhibitory activity but that have AKR1C3 inhibitory activity, methods for inhibiting AKR1C3 polypeptide biological activities, and methods for treating prostate tumors in subjects.
    Type: Grant
    Filed: February 19, 2018
    Date of Patent: September 3, 2019
    Assignees: Vanderbilt University, The Trustees of the University of Pennsylvania
    Inventors: Lawrence J. Marnett, Andy J. Liedtke, Trevor M. Penning, Adegoke O. Adeniji, Michael C. Byrns
  • Patent number: 10208033
    Abstract: The present invention relates to ?-carboline, dihydro-?-carboline and tetrahydro-?-carboline alkaloid derivatives (I) and a method for preparing same and the use in the aspects of preventing and treating plant viruses, fungicides and insecticides. For the meaning of each group in formula (I) see the description. The ?-carboline, dihydro-?-carboline and tetrahydro-?-carboline alkaloid derivatives of the present invention show a particularly ourstanding anti-plant virus activity, and also have fungicidal and insecticidal activities.
    Type: Grant
    Filed: December 24, 2014
    Date of Patent: February 19, 2019
    Assignees: NANKAI UNIVERSITY, NATIONAL PESTICIDE ENGINEERING RESEARCH CENTER (TIANJIN)
    Inventors: Qingmin Wang, Hongjian Song, Yongxian Liu, Yuxiu Liu
  • Patent number: 9616050
    Abstract: The invention concerns compounds of Formula (I) or pharmaceutically-acceptable salts thereof, wherein R1 to R5 have any of the meanings defined hereinbefore in the description; processes for their preparation, pharmaceutical compositions containing them and their use in the treatment of cell proliferative disorders.
    Type: Grant
    Filed: August 31, 2015
    Date of Patent: April 11, 2017
    Assignee: AstraZeneca AB
    Inventors: Robert Hugh Bradbury, David Buttar, Christopher De Savi, Craig Samuel Donald, Richard Albert Norman, Alfred Arthur Rabow, Gordon Stuart Currie, Heather Redfearn, Nadim Akhtar, Helen Elizabeth Williams, Matthew Osborne, Neda Yavari
  • Patent number: 9546167
    Abstract: This disclosure relates to a one-step method for preparing the tau radiopharmaceutical, [18F]T807, using an unprotected or protected precursor (e.g., tert-butyl 7-(6-nitropyridin-3-yl)-5H-pyrido[4,3-b]indole-5-carboxylate).
    Type: Grant
    Filed: March 31, 2016
    Date of Patent: January 17, 2017
    Assignee: The General Hospital Corporation
    Inventors: Neil Vasdev, Timothy M. Shoup
  • Patent number: 9169247
    Abstract: Certain 2-halophenyl, 2,4-dihalophenyl (e.g. 2,4-dichlorophenyl), 3,4-dichlorophenyl (e.g. 3,4-dichlorophenyl), 2,6-dichlorophenyl (2,6-dichlorophenyl) and 2,5-diakoxyphenyl (e.g. 2,5-dimethoxyphenyl) derivatives of tetrahydro-?-carbolines are provided, along with their pharmaceutically acceptable salts; prodrugs and solvates, and compositions containing the compounds. The compounds are useful for the prevention and treatment of cancer, and other indications where PDE5 inhibitors have shown benefits including erectile dysfunction, pulmonary hypertension, enhancing cognitive function, cystic fibrosis, or enhancing the activity of conventional chemotherapeutic drugs. Methods for fabricating the compounds are also provided.
    Type: Grant
    Filed: November 19, 2010
    Date of Patent: October 27, 2015
    Assignee: Southern Research Institute
    Inventors: Gary A. Piazza, Ashraf H. Abadi
  • Patent number: 9155727
    Abstract: The invention concerns compounds of Formula (I) or pharmaceutically-acceptable salts thereof, wherein R1 to R5 have any of the meanings defined hereinbefore in the description: processes for their preparation, pharmaceutical compositions containing them and their use in the treatment of cell proliferative disorders.
    Type: Grant
    Filed: May 27, 2014
    Date of Patent: October 13, 2015
    Assignee: AstraZeneca AB
    Inventors: Robert Hugh Bradbury, David Buttar, Christopher De Savi, Craig Samuel Donald, Richard Albert Norman, Alfred Arthur Rabow, Gordon Stuart Currie, Heather Marie Redfearn, Nadim Akhtar, Helen Elizabeth Williams, Matthew Osborne, Neda Yavari
  • Patent number: 9045471
    Abstract: A phosphorescent compound is represented by following Formula:
    Type: Grant
    Filed: October 28, 2011
    Date of Patent: June 2, 2015
    Assignee: LG Display Co., Ltd.
    Inventors: Hyoung-Yun Oh, In-Bum Song, Sung-Hee Park
  • Patent number: 9035056
    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. The compounds may bind to and antagonize receptor ?2B, ?1B or ?2A. 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, or 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. The compounds may also be used to treat diseases or conditions that are expected to be responsive to a decrease in blood pressure. Use of the compounds to treat cardiovascular, renal disorders or type 2 diabetes is particularly described.
    Type: Grant
    Filed: February 17, 2012
    Date of Patent: May 19, 2015
    Assignee: Medivation Technologies, Inc.
    Inventors: Sarvajit Chakravarty, Barry Patrick Hart, Rajendra Parasmal Jain
  • Patent number: 9034880
    Abstract: This disclosure relates to new tetracyclic compounds that may be used to modulate a histamine receptor in an individual. The compounds in one embodiment are tetracyclic [4,3-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: Grant
    Filed: March 8, 2013
    Date of Patent: May 19, 2015
    Assignee: Medivation Technologies, Inc.
    Inventors: David T. Hung, Andrew Asher Protter, Rajendra Parasmal Jain, Sundeep Dugar, Sarvajit Chakravarty
  • Patent number: 8999978
    Abstract: This disclosure relates to new tetracyclic compounds that may be used to modulate a histamine receptor in an individual. The compounds in one embodiment are tetracyclic [4,3-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: Grant
    Filed: November 16, 2012
    Date of Patent: April 7, 2015
    Assignee: Medivation Technologies, Inc.
    Inventors: David T. Hung, Andrew Asher Protter, Rajendra Parasmal Jain, Sundeep Dugar, Sarvajit Chakravarty
  • Publication number: 20150051204
    Abstract: Present invention refers to new compounds of formula I or II, its synthesis and its use in the treatment of metabolic syndrome, particularly for the treatment of type I or type II diabetes and/or metabolic syndrome or metabolic disease or metabolic disorders.
    Type: Application
    Filed: March 28, 2012
    Publication date: February 19, 2015
    Applicant: SJT MOLECULAR RESEARCH, S.L.
    Inventors: Juan Carlos Agreda Navajas, Roberto Mikio Kassuya
  • Publication number: 20150021555
    Abstract: Luminescent materials including donor-acceptor compounds with a high triplet energy heteropolyaromatic system, namely, dibenzofuran, dibenzothiophene and dibenzoselenophene with one or multiple nitrogens in the ring as the electron acceptor for use as emitters in organic light emitting diodes is disclosed.
    Type: Application
    Filed: July 16, 2013
    Publication date: January 22, 2015
    Inventors: Raymond Kwong, Chuanjun Xia, Scott Joseph, Siu Tung Lam, Chi Hang Lee
  • Publication number: 20150018369
    Abstract: The disclosure provides methods of treating glioblastoma, methods of screening for compounds that treat glioblastoma, and pharmaceutical compositions useful in the treatment of glioblastoma.
    Type: Application
    Filed: January 9, 2013
    Publication date: January 15, 2015
    Inventors: Nephi Stella, Philippe Diaz
  • Patent number: 8932557
    Abstract: Disclosed here in are compounds and methods of diagnosing Alzheimer's Disease or a predisposition thereto in a mammal, the method comprising administering to the mammal a diagnostically effective amount of a radiolabeled compound, wherein the compound is selected from the group consisting of radiolabeled carbazoles and derivatives thereof and triazoles derivatives, allowing the compound to distribute into the brain tissue, and imaging the brain tissue, wherein an increase in binding of the compound to the brain tissue compared to a normal control level of binding indicates that the mammal is suffering from or is at risk of developing Alzheimer's Disease.
    Type: Grant
    Filed: May 22, 2012
    Date of Patent: January 13, 2015
    Assignee: Eli Lilly and Company
    Inventors: Gang Chen, Umesh B. Gangadharmath, Dhanalakshmi Kasi, Anjana Sinha, Wei Zhang, Kai Chen, Vani P. Mocharla
  • Patent number: 8927570
    Abstract: Provided are 1-aryl or 1-heteroaryl substituted beta-carboline compounds or indole analogs thereof having the structure: where X is NH, N—C1-C4 alkyl, S, or O; R1 is 1-naphthyl or 1-dihydroacenaphthenyl, each optionally substituted with a halogen; and R2, R3, R4, R5, R6, and R7 are independently H H, OH, halogen, CN, C1-C4 alkyl, C1-C4 alkoxy, C1-C4 haloalkoxy, —C(O)OC1-C4 ester, —C1-C4—SO2—NH—C1-C4 sulfonamide, or phenyl with the proviso that X is NH, R1 is 1-naphthyl or 1-naphthyl substituted with a halogen and one of R5, R6, or R7 is C1-C4 alkoxy, then R2, R3, R4, R5, R6, and R7 are independently H, OH, halogen, CN, C1-C4 haloalkoxy, —C(O)OC1-C4 ester, —C1-C4—SO2—NH—C1-C4 sulfonamide, or phenyl such that at least two of R2, R3, R4, R5, R6, and R7 are other than H. Also provided are methods for inhibiting proliferation of cells associated with a cell proliferative disease by contacting the cell with the compounds provided herein.
    Type: Grant
    Filed: October 30, 2012
    Date of Patent: January 6, 2015
    Inventor: John K. Buolamwini
  • Publication number: 20140357661
    Abstract: The invention concerns compounds of Formula (I) or pharmaceutically-acceptable salts thereof, wherein R1 to R5 have any of the meanings defined hereinbefore in the description: processes for their preparation, pharmaceutical compositions containing them and their use in the treatment of cell proliferative disorders.
    Type: Application
    Filed: May 27, 2014
    Publication date: December 4, 2014
    Applicant: ASTRAZENECA AB
    Inventors: Robert Hugh BRADBURY, David BUTTAR, Christopher DE SAVI, Craig Samuel DONALD, Richard Albert NORMAN, Alfred Arthur RABOW, Gordon Stuart CURRIE, Heather Marie REDFEARN, Nadim AKHTAR, Helen Elizabeth WILLIAMS, Matthew OSBORNE, Neda YAVARI
  • Patent number: 8871798
    Abstract: This disclosure relates to compounds of formula I: wherein R1, R2, R3, R4, X and Y have the meanings denoted in the disclosure. The compounds of formula I have antithrombotic activity and in particular inhibit the protease-activated receptor 1 (PAR1). The disclosure further relates to a method for producing the compound of formula I and to the use thereof as a pharmaceutical product.
    Type: Grant
    Filed: October 16, 2012
    Date of Patent: October 28, 2014
    Assignee: Sanofi
    Inventors: Karl Schoenafinger, Henning Steinhagen, Bodo Scheiper, Uwe Heinelt, Volkmar Herrmann, Matthias Herrmann
  • 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
  • Publication number: 20140288068
    Abstract: In one aspect, the invention provides compounds of Formula I, and salts, hydrates and isomers thereof. In another aspect, the invention provides a method of promoting bone formation in a subject in need thereof by administering to the subject a therapeutically effective amount of a compound of Formula I, Formula II, or Formula III. The present invention also provides orthopedic and periodontal devices, as well as methods for the treatment of renal disease and cancer, using a compound of Formula I, Formula II, or Formula III.
    Type: Application
    Filed: March 14, 2014
    Publication date: September 25, 2014
    Applicant: OssiFi Inc.
    Inventors: Debra Ellies, Jean-Philippe Rey, F. Scott Kimball
  • Patent number: 8841318
    Abstract: The present invention provides substituted tricyclic heteroaryl compounds, including, for example, pyridoindoles, pyrimidinoindoles and triazinoindoles that modulate the activity of Janus kinases and are useful in the treatment of diseases related to activity of Janus kinases such as immune-related diseases, skin disorders, myeloid proliferative disorders, cancer, and other diseases.
    Type: Grant
    Filed: March 15, 2013
    Date of Patent: September 23, 2014
    Assignee: Incyte Corporation
    Inventors: Argyrios G. Arvanitis, James D. Rodgers, Louis Storace, Beverly Folmer
  • 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
  • Publication number: 20140231794
    Abstract: A compound represented by the following formula (1): wherein in the formula (1), Ar1 and Ar2 are independently a substituted or unsubstituted aryl group, a substituted or unsubstituted heteroaryl group, or a substituted or unsubstituted alkyl group; X1 to X4 and X13 to X16 are independently CR1, CH or N; one of X5 to X8 is a carbon atom bonding to one of X9 to X12, and at least one of X5 to X8 that is adjacent to the carbon atom bonding to one of X9 to X12 is CR2; one of X9 to X12 is a carbon atom bonding to one of X5 to X8, and X9 to X12 that is adjacent to the carbon atom bonding to one of X5 to X8 is CH or N; and the remaining X5 to X8 and the remaining X9 to X12 are CR1, CH or N.
    Type: Application
    Filed: September 25, 2012
    Publication date: August 21, 2014
    Applicant: Idemitsu Kosan Co., Ltd.
    Inventors: Toshihiro Iwakuma, Kei Yoshida
  • 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: 20140206711
    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. The compounds may bind to and antagonize receptor ?2B, ?1B or ?2A. 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, or 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. The compounds may also be used to treat diseases or conditions that are expected to be responsive to a decrease in blood pressure. Use of the compounds to treat cardiovascular, renal disorders or type 2 diabetes is particularly described.
    Type: Application
    Filed: February 17, 2012
    Publication date: July 24, 2014
    Applicant: Medivation Technologies, Inc.
    Inventors: Sarvajit Chakravarty, Barry Patrick Hart, Rajendra Parasmal Jain
  • Patent number: 8779139
    Abstract: The present invention provides methods for the preparation of substituted 2,3,4,4a,5,9b-hexahydro-1H-pyrido[4,3-b]indole derivative useful as intermediates and methods for producing and using such intermediates.
    Type: Grant
    Filed: August 23, 2012
    Date of Patent: July 15, 2014
    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
  • Publication number: 20140194414
    Abstract: This disclosure relates to new tetracyclic compounds that may be used to modulate a histamine receptor in an individual. The compounds in one embodiment are tetracyclic[4,3-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: March 8, 2013
    Publication date: July 10, 2014
    Applicant: MEDIVATION TECHNOLOGIES, INC.
    Inventor: MEDIVATION TECHNOLOGIES, INC.
  • Patent number: 8765760
    Abstract: Provided herein are compounds of formula (I): A-L-B??(I) and pharmaceutically acceptable salts and stereoisomers thereof, wherein A is wherein X is (i) CR1 or N, or (ii) O or NR2, each Y is independently N or CR3, and each Z is independently N or C, wherein R1, R2 and R3 are defined in the specification; L is a linker, and B is a multicyclic ring; methods of their synthesis, pharmaceutical compositions comprising the compounds, and methods of their use. The compounds provided herein are inhibitors of phosphodiesterases and useful for the treatment, prevention, and/or management of various disorders, such as CNS disorders and metabolic disorders, e.g., neurological disorders, psychosis, schizophrenia, obesity and diabetes.
    Type: Grant
    Filed: January 10, 2012
    Date of Patent: July 1, 2014
    Assignee: Sunovion Pharmaceuticals, Inc.
    Inventors: John Emmerson Campbell, Philip Jones, Michael Charles Hewitt
  • Publication number: 20140100242
    Abstract: Methods are provided for identifying molecules that can be used to positively and negatively manipulate quorum-sensing-mediated communication to control bacterial behavior. Small-molecule antagonists that disrupt quorum-sensing-mediated activities are identified. Methods are provided for disrupting detection of acyl-homoserine lactone autoinducer in Gram-negative bacteria by contacting the bacteria with the antagonists. Methods of inhibiting quorum sensing-mediated activity in Gram-negative bacteria are provided wherein the activity is pathogenicity, bioluminescence, siderophore production, type III secretion, or metalloprotease production.
    Type: Application
    Filed: September 17, 2013
    Publication date: April 10, 2014
    Applicant: THE TRUSTEES OF PRINCETON UNIVERSITY
    Inventors: Bonnie Bassler, Lee Swem
  • Patent number: 8673933
    Abstract: The present invention provides compounds of formula I and pharmaceutically acceptable salts thereof. The formula I compounds inhibit tyrosine kinase activity of JAK2, thereby making them useful as antiproliferative agents for the treatment of cancer and other diseases.
    Type: Grant
    Filed: April 30, 2012
    Date of Patent: March 18, 2014
    Assignee: Bristol-Myers Squibb Company
    Inventors: Ashok V. Purandare, James W. Grebinski, Amy C. Hart, Jennifer Inghrim, Gretchen M. Schroeder, Honghe Wan
  • Publication number: 20130341604
    Abstract: The present invention provides an organic compound having excellent properties, which is excellent in electron-injection/transport performance, has hole-blocking ability and is high stability in a thin-film state, as a material for an organic electroluminescence device having a high efficiency and a high durability, and provides is an organic electroluminescence device having a high efficiency and a high durability using the compound. The present invention relates to a compound having a substituted anthracene ring structure and a pyridoindole ring structure represented by general formula (1); and an organic electroluminescence device having a pair of electrodes and at least one organic layer interposed between the electrodes in which the at least one organic layer contains the compound.
    Type: Application
    Filed: June 18, 2013
    Publication date: December 26, 2013
    Inventors: Norimasa YOKOYAMA, Shuichi Hayashi, Sawa Izumi, Naoaki Kabasawa, Shigeru Kusano
  • Patent number: 8568756
    Abstract: Methods are provided for identifying molecules that can be used to positively and negatively manipulate quorum-sensing-mediated communication to control bacterial behavior. Small-molecule antagonists that disrupt quorum-sensing-mediated activities are identified. Methods are provided for disrupting detection of acyl-homoserine lactone autoinducer in Gram-negative bacteria by contacting the bacteria with the antagonists. Methods of inhibiting quorum sensing-mediated activity in Gram-negative bacteria are provided wherein the activity is pathogenicity, bioluminescence, siderophore production, type III secretion, or metalloprotease production.
    Type: Grant
    Filed: June 2, 2009
    Date of Patent: October 29, 2013
    Assignee: The Trustees of Princeton University
    Inventors: Bonnie Bassler, Lee Swem
  • Publication number: 20130274258
    Abstract: Compounds of general formula (I), wherein A, Y, R1 and R2 are defined herein are useful in the treatment or prevention of proliferative diseases including cancer or infectious or parasitic diseases.
    Type: Application
    Filed: November 3, 2011
    Publication date: October 17, 2013
    Applicant: PHILIP MORRIS PRODUCTS S.A.
    Inventors: Stephane Demotz, Gerhard Lang, Damian McHugh, Axel Teichert, Fernando Goffman, Paul M. Doyle, Paul M. Blaney, Raymond Fisher, Andrew Smith, Emma L. Blaney, Simon Foster
  • 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
  • Patent number: 8546420
    Abstract: The present invention relates to 4,5-ring annulated indole derivatives of formula (I), compositions comprising at least one 4,5-ring annulated indole derivatives, and methods of using the 4,5-ring annulated indole derivatives for treating or preventing a viral infection or a virus-related disorder in a patient, wherein ring Z of formula (I), is cyclohexyl, cyclohexenyl, 6-membered heterocycloalkyl, 6-membered heterocycloalkenyl, 6-membered aryl or 6-membered heteroaryl, wherein R1, R2, R3, R6, R7 and R10 are as described herein.
    Type: Grant
    Filed: December 17, 2007
    Date of Patent: October 1, 2013
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Gopinadhan N. Anilkumar, Yueheng Jiang, Stuart B. Rosenblum, Srikanth Venkatraman, Francisco Velazquez, Neng-Yang Shih, F. George Njoroge, Joseph A. Kozlowski
  • Publication number: 20130203746
    Abstract: This disclosure relates to new tetracyclic compounds that may be used to modulate a histamine receptor in an individual. The compounds in one embodiment are tetracyclic [4,3-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: November 16, 2012
    Publication date: August 8, 2013
    Inventor: Medivation Technologies Inc.
  • Publication number: 20130190323
    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: 20130190347
    Abstract: This disclosure relates to new tricyclic compounds that may be used to modulate a histamine receptor in an individual. Compounds are described, including new 2,3,4,5-tetrahydro-1H-pyrido[4,3-b]indole compounds. 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: March 7, 2013
    Publication date: July 25, 2013
    Applicant: MEDIVATION TECHNOLOGIES, INC.
    Inventor: Medivation Technologies, Inc.
  • Publication number: 20130190322
    Abstract: This disclosure is directed to pyrido[4,3-b]indoles having rigid moieties. The compounds in one embodiment are pyrido[4,3-b]indoles having an unsaturated hydrocarbon moiety. The compounds in another embodiment are pyrido[4,3-b]indoles having a cycloalkyl, cycloalkenyl or heterocyclyl moiety. 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: 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: 20130190328
    Abstract: New heterocyclic compounds that may be used to modulate a histamine receptor in an individual are described. 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: 20130190331
    Abstract: New heterocyclic compounds that may be used to modulate a histamine receptor in an individual are described. 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: 20130190304
    Abstract: This disclosure relates to new tetracyclic compounds that may be used to modulate a histamine receptor in an individual. The compounds in one embodiment are tetracyclic [4,3-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: March 12, 2013
    Publication date: July 25, 2013
    Applicant: MEDIVATION TECHNOLOGIES, INC.
    Inventor: Medivation Technologies, Inc.
  • Publication number: 20130190348
    Abstract: This disclosure relates to new tricyclic compounds that may be used to modulate a histamine receptor in an individual. Compounds are described, including new 2,3,4,5-tetrahydro-1H-pyrido[4,3-b]indole compounds. 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: March 8, 2013
    Publication date: July 25, 2013
    Applicant: MEDIVATION TECHNOLOGIES, INC.
    Inventor: MEDIVATION TECHNOLOGIES, INC.
  • Patent number: 8476294
    Abstract: The invention relates to the use of 1H-imidazo[4,5-c]quinolinone derivatives and salts thereof in the treatment of protein and/or lipid kinase dependent diseases and for the manufacture of pharmaceutical preparations for the treatment of said diseases; 1H-imidazo[4,5-c]quinolinone derivatives for use in the treatment of protein and/or lipid kinase dependent diseases; a method of treatment against said diseases, comprising administering the 1H-imidazo[4,5-c]quinolinone derivatives to a warm-blooded animal, especially a human; pharmaceutical preparations comprising an 1H-imidazo[4,5-c]quinolinone derivative, especially for the treatment of a protein and/or lipid kinase dependent disease; novel 1H-imidazo[4,5-c]quinolinone derivatives; and a process for the preparation of the novel 1H-imidazo[4,5-c]quinolinone derivatives.
    Type: Grant
    Filed: June 2, 2010
    Date of Patent: July 2, 2013
    Assignee: Novartis AG
    Inventors: Pascal Furet, Frank Stephan Kalthoff, Robert Mah, Christian Ragot, Frédéric Stauffer
  • Patent number: 8471008
    Abstract: A material for organic electroluminescence devices for use as a host material in combination with at least one phosphorescent metal complex, which comprises a compound having a specific heterocyclic structure, is described. Also described is an organic electroluminescence device having an anode, a cathode and an organic thin film layer having one or more layers. The organic thin film layer is interposed between the anode and cathode and has a light emitting layer containing a host material in combination with at least one phosphorescent metal complex. At least one layer of the organic thin film layer contains the material for organic electroluminescence devices. The material for organic electroluminescence devices provides an organic electroluminescence device which has a high emitting efficiency, causes little pixel defects, is excellent in heat resistance, and show a long lifetime.
    Type: Grant
    Filed: November 25, 2011
    Date of Patent: June 25, 2013
    Assignee: Idemitsu Kosan Co., Ltd.
    Inventors: Toshihiro Iwakuma, Jun Endo, Masaki Numata, Kenichi Fukuoka
  • Publication number: 20130137705
    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: September 23, 2010
    Publication date: May 30, 2013
    Inventor: Sarvajit Chakravarty
  • Publication number: 20130131077
    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: December 21, 2012
    Publication date: May 23, 2013
    Applicant: Medivation Technologies, Inc.
    Inventor: Medivation Technologies, Inc.
  • Publication number: 20130131070
    Abstract: Provided are 1-aryl or 1-heteroaryl substituted beta-carboline compounds or indole analogs thereof having the structure: where X is NH, N—C1-C4 alkyl, S, or O; R1 is 1-naphthyl or 1-dihydroacenaphthenyl, each optionally substituted with a halogen; and R2, R3, R4, R5, R6, and R7 are independently H H, OH, halogen, CN, C1-C4 alkyl, C1-C4 alkoxy, C1-C4 haloalkoxy, —C(O)OC1-C4 ester, —C1-C4—SO2—NH—C1-C4 sulfonamide, or phenyl with the proviso that X is NH, R1 is 1-naphthyl or 1-naphthyl substituted with a halogen and one of R5, R6, or R7 is C1-C4 alkoxy, then R2, R3, R4, R5, R6, and R7 are independently H, OH, halogen, CN, C1-C4 haloalkoxy, —C(O)OC1-C4 ester, —C1-C4—SO2—NH—C1-C4 sulfonamide, or phenyl such that at least two of R2, R3, R4, R5, R6, and R7 are other than H. Also provided are methods for inhibiting proliferation of cells associated with a cell proliferative disease by contacting the cell with the compounds provided herein.
    Type: Application
    Filed: October 30, 2012
    Publication date: May 23, 2013
    Inventor: John K. Buolamwini