Four Or More Ring Nitrogens In The Polycyclo Ring System Patents (Class 544/81)
  • Patent number: 9359361
    Abstract: The present invention relates to a compound of Formula I: or a pharmaceutically acceptable salt thereof, wherein the symbols are as defined in the specification; a pharmaceutical composition comprising the same; and a method for treating or preventing autoimmunity disease using the same.
    Type: Grant
    Filed: June 1, 2012
    Date of Patent: June 7, 2016
    Assignee: JANUS BIOTHERAPEUTICS, INC.
    Inventors: Grayson B. Lipford, Charles M. Zepp
  • Publication number: 20150051202
    Abstract: Compounds of the formula I in which R1, R2 and R4 have the meanings indicated in Claim 1, are inhibitors of GCN2, and can be employed, inter alia, for the treatment of cancer.
    Type: Application
    Filed: February 14, 2013
    Publication date: February 19, 2015
    Applicant: Merck Patent GmbH
    Inventors: Kai Schiemann, Carl Deutsch, Guenter Hoelzemann, Daniel Kuhn, Ansgar Wegener, Dominique Swinnen, Horacio Comas
  • Publication number: 20150038462
    Abstract: A method of inhibiting replication of a flavivirus in animal cells, and an oligonucleotide compound for use in the method are disclosed. The oligonucleotide analog (i) has a nuclease-resistant backbone, (ii) is capable of uptake by the cells, (iii) contains between 8-40 nucleotide bases, and (iv) has a sequence of at least 8 bases complementary to a region of the virus' positive strand RNA genome that includes at least a portion of SEQ ID NOS:1-4. Exposure of cells infected with a flavivirus to the analog is effective to form within the cells, a heteroduplex structure composed of the virus ssRNA and the oligonucleotide, characterized by a Tm of dissociation of at least 45° C., and having disrupted base pairing between the virus's 5? and 3? cyclization sequences.
    Type: Application
    Filed: December 11, 2013
    Publication date: February 5, 2015
    Applicant: Sarepta Therapeutics, Inc.
    Inventors: Patrick L. Iversen, David A. Stein
  • Patent number: 8940736
    Abstract: The invention provides compounds of Formula (I) and pharmaceutically acceptable salts thereof. The Formula (I) imidazotriazines inhibit protein kinase activity thereby making them useful as anticancer agents.
    Type: Grant
    Filed: July 12, 2013
    Date of Patent: January 27, 2015
    Assignee: Bristol-Myers Squibb Company
    Inventors: Ashok Vinayak Purandare, Brian E. Fink, Ashvinikumar V. Gavai, Walter Lewis Johnson, Amy C. Hart, Liqi He, Tram N. Huynh, Jennifer Inghrim, Harold Mastalerz, Xiaopeng Sang, Christine M. Tarby, Honghe Wan, Wayne Vaccaro, Guifen Zhang, Yufen Zhao, Kurt Zimmermann
  • Publication number: 20150025058
    Abstract: Compounds of the formula I in which R1, R2 and R4 have the meanings indicated in Claim 1, are inhibitors of Syk, and can be employed, inter alia, for the treatment of cancer, rheumatoid arthritis and/or systemic lupus
    Type: Application
    Filed: January 22, 2013
    Publication date: January 22, 2015
    Applicant: MERCK PATENT GMBH
    Inventors: Carl Deutsch, Daniel Kuhn, Tatjana Ross, Lars Burgdorf
  • Publication number: 20140221646
    Abstract: The present invention relates to a compound of Formula I: or a pharmaceutically acceptable salt thereof, wherein the symbols are as defined in the specification; a pharmaceutical composition comprising the same; and a method for treating or preventing autoimmunity disease using the same.
    Type: Application
    Filed: February 12, 2014
    Publication date: August 7, 2014
    Applicant: JANUS BIOTHERAPEUTICS, INC.
    Inventors: Grayson B. LIPFORD, Charles M. ZEPP
  • Publication number: 20140155813
    Abstract: To provide a technology for introducing a PMO with remarkably enhanced cell permeability, leading to significantly enhanced introduction efficiency to thereby provide a therapeutic drug that dramatically ameliorates a medical condition of DMD. Also provided is a therapeutic drug for Duchenne muscular dystrophy, including as an active ingredient a Bubble liposome having a specific morpholino oligomer (PMO) bound to a surface thereof, in which the PMO is introduced into a muscle fiber (muscle cell) of a muscle tissue with high efficiency by administration of the therapeutic drug into the muscle tissue or into a blood vessel followed by ultrasound irradiation to the muscle tissue transcutaneously.
    Type: Application
    Filed: April 25, 2012
    Publication date: June 5, 2014
    Applicant: NEPA GENE CO., LTD.
    Inventors: Yoichi Negishi, Yoko Takahashi, Kazuo Maruyama, Yukihiko Aramaki
  • Publication number: 20140135315
    Abstract: There is provided a compound of formula I: or a pharmaceutically acceptable salt thereof. There are also provided processes for the manufacture of a compound of Formula 1, and the use of a compound of Formula 1 as a medicament and in the treatment of cancer.
    Type: Application
    Filed: April 9, 2013
    Publication date: May 15, 2014
    Applicant: KuDOS Pharmaceuticals Limited
    Inventor: KuDOS Pharmaceuticals Limited
  • Publication number: 20140018319
    Abstract: The invention provides compounds of Formula (I) and pharmaceutically acceptable salts thereof. The Formula (I) imidazotriazines inhibit protein kinase activity thereby making them useful as anticancer agents.
    Type: Application
    Filed: July 12, 2013
    Publication date: January 16, 2014
    Inventors: Ashok Vinayak Purandare, Brian E. Fink, Ashvinikumar V. Gavai, Walter Lewis Johnson, Amy C. Hart, Liqi He, Tram N. Huynh, Jennifer Inghrim, Harold Mastalerz, Xiaopeng Sang, Christine M. Tarby, Honghe Wan, Wayne Vaccaro, Guifen Zhang, Yufen Zhao, Kurt Zimmermann
  • Publication number: 20130289091
    Abstract: A method and antisense compound for inhibiting the growth of pathogenic bacterial cells are disclosed. The compound contains no more than 12 nucleotide bases and has a targeting nucleic acid sequence of no fewer than 10 bases in length that is complementary to a target sequence containing or within 10 bases, in a downstream direction, of the translational start codon of a bacterial mRNA that encodes a bacterial protein essential for bacterial replication. The compound binds to a target mRNA with a Tm of between 50° to 60° C. The relatively short antisense compounds are substantially more active than conventional antisense compounds having a targeting base sequence of 15 or more bases.
    Type: Application
    Filed: November 19, 2012
    Publication date: October 31, 2013
    Inventors: Bruce L. Geller, Jesse D. Deere, Patrick L. Iversen
  • Patent number: 8445487
    Abstract: Purine compounds of Formula I, and including stereoisomers, geometric isomers, tautomers, solvates, metabolites and pharmaceutically acceptable salts thereof, are useful for inhibiting lipid kinases including p110 alpha and other isoforms of PI3K, and for treating disorders such as cancer mediated by lipid kinases. Methods of using compounds of Formula I for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed.
    Type: Grant
    Filed: February 9, 2012
    Date of Patent: May 21, 2013
    Assignee: Genentech, Inc.
    Inventors: Georgette Castanedo, Irina Chuckowree, Adrian Folkes, Daniel P. Sutherlin, Nan Chi Wan
  • Publication number: 20130085139
    Abstract: Certain disclosed oligomers induce exon skipping during processing of myostatin pre-mRNA. The oligomers may be in a vector or encoded by the vector. The vector is used for inducing exon skipping during processing of myostatin pre-mRNA. A therapeutically effective amount of the oligomer may be administered to a subject patient such that exon skipping during processing of myostatin pre-mRNA is induced. The administration to a subject may be used in order to increase or maintain muscle mass, or slowing degeneration of muscle mass in the subject. The administration to a subject may ameliorate muscle wasting conditions, such as muscular dystrophy.
    Type: Application
    Filed: October 4, 2012
    Publication date: April 4, 2013
    Applicant: ROYAL HOLLOWAY AND BEDFORD NEW COLLEGE
    Inventor: Royal Holloway and Bedford New College
  • Publication number: 20130053371
    Abstract: There is provided compounds of formula (I), wherein A1, A4, A4a, A5, B1, B1a, B2, B2a, B3, B3a, B4, B4a and R3 have meanings given in the description, and pharmaceutically-acceptable esters, amides, solvates or salts thereof, which compounds are useful in the treatment of diseases in which inhibition of a protein or lipid kinase (e.g. a PI3-K and/or mTOR) is desired and/or required, and particularly in the treatment of cancer or a proliferative disease.
    Type: Application
    Filed: January 24, 2011
    Publication date: February 28, 2013
    Applicant: CENTRO NACIONAL DE INVESTIGACIONES ONCOLÓGICAS (CNIO)
    Inventors: Joaquin Pastor Fernández, Sonia Martinez Gonzalez, Rosa Maria Alvarez Escobar, Antonlo Rodriguez Hergueta, José Ignacio Martin Hernando, Francisco Ramos Lima
  • Publication number: 20130053556
    Abstract: Morpholinos are widely used to block the activity of selected single-stranded genetic sequences. This invention comprises Morpholinos containing one or more integral photolinkers (Photo-Morpholinos) wherein the photolinkers are directly incorporated into the sequence of a Morpholino, where the photolinker has a size and structure which emulates the size and structure of a Morpholino subunit. This integrated photolinker design substantially simplifies and reduces cost of production relative to earlier photocleavable compositions. The invention also comprises use of these Photo-Morpholinos for modulating the expression of any selected gene transcript at any selected time and at any selected site simply by exposure to light. These Photo-Morpholinos afford a new use wherein a gene transcript is rendered inactive by contacting with a Photo-Morpholino—and then later exposure to light cleaves the Photo-Morpholino to inactive fragments—thereby reactivating that previously inactivated gene transcript.
    Type: Application
    Filed: August 26, 2011
    Publication date: February 28, 2013
    Applicant: GENE TOOLS, LLC
    Inventors: Yong-Fu Li, James E. Summerton, Paul A. Morcos
  • Patent number: 8299206
    Abstract: Improved methods are described for solid-phase synthesis of morpholino oligomers, in which a protected morpholino ring nitrogen is deprotected between coupling steps using a heterocyclic amine salt in a trifluoroethanol-containing solvent, where the salt is a salt of a heterocyclic amine, having a pKa in the range of 1-4 in its protonated form, with an acid selected from a sulfonic acid, trifluoroacetic acid, and hydrochloric acid. Examples are 3-chloropyridinium methanesulfonate (CPM) and 4-cyanopyridinium trifluoroacetate (CYTFA).
    Type: Grant
    Filed: November 14, 2008
    Date of Patent: October 30, 2012
    Assignee: AVI BioPharma, Inc.
    Inventors: Christina Mary Josephine Fox, Dwight D. Weller
  • Publication number: 20120220576
    Abstract: The invention relates to novel heterocyclic compounds of the formula in which all of the variables are as defined in the specification, to their preparation, to their medical use, in particular to their use in the treatment of cancer and neurodegenerative disorders, and to medicaments comprising them.
    Type: Application
    Filed: January 30, 2012
    Publication date: August 30, 2012
    Inventors: Branko RADETICH, Bing YU, Yanyi ZHU
  • Publication number: 20120208808
    Abstract: Compounds of the formula (I), in which X, R1 and R2 have the meanings indicated in claim 1, are PI3K inhibitors and can be employed, inter alia, for the treatment of autoimmune diseases, inflammation, cardiovascular diseases, neurodegenerative diseases and tumours.
    Type: Application
    Filed: September 24, 2010
    Publication date: August 16, 2012
    Applicant: MERCK PATENT GESELLSCHAFT MIT BESCHRANKTER HAFTUNG
    Inventors: Hans Peter Buchstaller, Ulrich Emde, Markus Klein, Christina Esdar, Joerg Bomke
  • Patent number: 8227598
    Abstract: The invention relates to novel heteroaryl carboxamides, a process for their preparation, and pharmaceutical compositions containing them. These materials are useful for the treatment and/or prophylaxis of diseases and for improving perception, concentration, learning and/or memory.
    Type: Grant
    Filed: August 10, 2007
    Date of Patent: July 24, 2012
    Assignee: Bayer Schering Pharma Aktiengesellschaft
    Inventors: Martin Hendrix, Frank-Gerhard Böβ, Christina Erb, Joachim Krüger, Christoph Methfessel, Rudy Schreiber, Welf-Burkhard Wiese, Joachim Luithle
  • Publication number: 20120157430
    Abstract: The present invention provides N-(1-(substituted-phenyl)ethyl)-9H-purin-6-amines derivatives that modulate the activity of phosphoinositide 3-kinases (PI3Ks) and are useful in the treatment of diseases related to the activity of PI3Ks including, for example, inflammatory disorders, immune-based disorders, cancer, and other diseases.
    Type: Application
    Filed: December 19, 2011
    Publication date: June 21, 2012
    Inventors: Yun-Long Li, Andrew P. Combs, Eddy W. Yue, Thomas P. Maduskuie, JR., Richard B. Sparks
  • Publication number: 20120142673
    Abstract: There is provided a compound of formula I: or a pharmaceutically acceptable salt thereof. There are also provided processes for the manufacture of a compound of Formula 1, and the use of a compound of Formula 1 as a medicament and in the treatment of cancer.
    Type: Application
    Filed: November 30, 2011
    Publication date: June 7, 2012
    Applicant: KuDOS PHARMACEUTICALS LIMITED
    Inventors: Heather Mary Ellen Duggan, Frederic Georges Marie Leroux, Karine Malagu, Niall Morrison Barr Martin, Keith Allan Menear, Graeme Cameron Murray Smith
  • Patent number: 8193164
    Abstract: A compound of formula (I), or stereoisomers or pharmaceutically acceptable salts thereof, wherein, R1a, R1b, R2a, R2b, U1, U2, X1, X2 and L are as defined herein.
    Type: Grant
    Filed: April 19, 2007
    Date of Patent: June 5, 2012
    Assignee: Novartis AG
    Inventors: Robin Alec Fairhurst, Roger John Taylor
  • Patent number: 8188095
    Abstract: The present invention relates to compounds which inhibit bacterial gyrase and/or Topo IV and pharmaceutically acceptable compositions comprising said compounds. These compounds, and compositions thereof, are useful in treating bacterial infection. Accordingly, the present invention also relates to methods for treating bacterial infections in mammals.
    Type: Grant
    Filed: October 7, 2008
    Date of Patent: May 29, 2012
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: Paul Charifson, David Deininger, Anne-Laure Grillot, Yusheng Liao, Steven Ronkin, Dean Stamos, Emanuele Perola, Tiansheng Wang, Arnaud Le Tiran, Joseph Drumm
  • Publication number: 20120094975
    Abstract: The present invention encompasses compounds of general formula (1) wherein the groups R1 to R4, X1, X1, X3, L1 and L2 are defined as in claim 1, which are suitable for the treatment of diseases characterised by excessive or anomalous cell pro-liferation, and the use thereof in such a treatment.
    Type: Application
    Filed: September 8, 2009
    Publication date: April 19, 2012
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: Andreas Mantoulidis, Georg Dahmann, Peter Ettmayer, Christian Klein, Steffen Steurer, Irene Waizenegger, Stephan Karl Zahn
  • Patent number: 8158624
    Abstract: Purine compounds of Formula I, and including stereoisomers, geometric isomers, tautomers, solvates, metabolites and pharmaceutically acceptable salts thereof, are useful for inhibiting lipid kinases including p110 alpha and other isoforms of PI3K, and for treating disorders such as cancer mediated by lipid kinases. Methods of using compounds of Formula I for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed.
    Type: Grant
    Filed: May 29, 2009
    Date of Patent: April 17, 2012
    Assignee: Genetech, Inc.
    Inventors: Georgette Castanedo, Irina Chuckowree, Adrian Folkes, Daniel P. Sutherlin, Nan Chi Wan
  • Publication number: 20120010203
    Abstract: The invention relates to novel compounds of formula I where R1, R2, R3, R4, R5, R6, R7, R8, Q1, Q2 and Q3 are each as defined below. The compounds of formula I have antithrombotic activity and inhibit especially protease-activated receptor 1 (PAR1). The invention further relates to a process for preparing the compound of formula I and to the use thereof as a medicament.
    Type: Application
    Filed: September 23, 2011
    Publication date: January 12, 2012
    Applicant: SANOFI-AVENTIS
    Inventors: Uwe HEINELT, Volkmar WEHNER, Matthias HERRMANN, Karl SCHOENAFINGER, Henning STEINHAGEN, Bodo SCHEIPER
  • Patent number: 8071609
    Abstract: This invention relates to compounds of the general formula: in which Q is an ethynyl or ethenyl moiety; Ring A is an aryl, heteroaryl or heterocyclic ring or ring system; and the remaining variable groups are as defined herein, and to their preparation and use.
    Type: Grant
    Filed: August 11, 2006
    Date of Patent: December 6, 2011
    Assignee: ARIAD Pharmaceuticals, Inc.
    Inventors: Yihan Wang, Wei-Sheng Huang, Rajeswari Sundaramoorthi, Xiaotian Zhu, R. Mathew Thomas, William C. Shakespeare, David C. Dalgarno, Tomi K. Sawyer
  • Patent number: 8067411
    Abstract: The present invention provides compounds of formula wherein R1, Y1, X1, Z1, X2, Y2, A, n and R2 are as defined in the specification, processes for their preparation, pharmaceutical compositions containing them and their use in therapy.
    Type: Grant
    Filed: December 13, 2007
    Date of Patent: November 29, 2011
    Assignees: AstraZeneca AB, Dainippon Sumitomo Pharma Co., Ltd.
    Inventors: Roger Victor Bonnert, Thomas McInally, Tobias Mochel, Stephen Thom
  • Publication number: 20110281857
    Abstract: 6-morpholin-4-yl-pyrazolo[3,4-d]pyrimidine and 2-morpholin-4-yl-7H-pyrrolo[2,3-d]pyrimidine derivatives have unexpected drug properties as inhibitors of PI3 and/or mTOR kinases and are useful in treating disorders related to abnormal PI3K/mTOR activities such as cancer, immune disorders, cardiovascular disease, viral infection, inflammation, metabolism/endocrine disorders and neurological disorders.
    Type: Application
    Filed: November 11, 2009
    Publication date: November 17, 2011
    Applicant: XCOVERY HOLDING COMPANY, LLC
    Inventors: Congxin Liang, Zhigang Li
  • Publication number: 20110230464
    Abstract: This invention provides a compound which is a purine of formula (Ia) or (Ib): and the pharmaceutically acceptable salts thereof that are inhibitors of PI3K and a selective for the p110? isoform, which is a class Ia PI3 kinase, over other class Ia PI3 kinases and over class Ib kinases. The compounds may be used to treat diseases and disorders arising from abnormal cell growth, function or behaviour associated with PI3 kinase such as cancer immune disorders, cardiovascular disease, viral infection, inflammation, metabolism/endocrine function disorders and neurological disorders.
    Type: Application
    Filed: October 27, 2008
    Publication date: September 22, 2011
    Inventors: Paul Goldsmith, Timothy Colin Hancox, Nei Anthony Pegg, Janusz Josef Kulagowski, Alan John Nadin, Stephen Price
  • Publication number: 20110190287
    Abstract: Novel compounds comprising a guanidine-rich head covalently coupled to one or more oligonucleotide antisense sequences which are useful to modulate blood coagulation by affecting the expression of integrin ?IIb or ?3 are described herein. This invention also includes pharmaceutical compositions containing these compounds, with or without other therapeutic agents, and to methods of using these compounds as inhibitor of platelet aggregation, as thrombolytics, and/or for the treatment of other thromboembolic disorders. Vivo-MOs, which include eight guanidine groups dendrimerically arranged in the guanidine-rich head and two synthetic antisense morpholino oligonucleotides, are representative compounds of the present invention.
    Type: Application
    Filed: January 28, 2011
    Publication date: August 4, 2011
    Applicant: University of North Texas
    Inventor: Pudur Jagadeeswaran
  • Publication number: 20110172418
    Abstract: The present invention provides an improved method for reducing the risk or severity of restenosis following cardiac angioplasty. The method includes administering to a target vessel region, a morpholino antisense compound having a phosphorus-containing backbone linkages, and spanning the start codon of a human c-myc mRNA. Also disclosed are novel antisense compounds and compositions, and a method for assaying the effectiveness of antisense delivery and uptake to a target vessel region.
    Type: Application
    Filed: August 11, 2010
    Publication date: July 14, 2011
    Applicant: AVI BIOPHARMA, INC.
    Inventors: PATRICK L. IVERSEN, DWIGHT D. WELLER
  • Publication number: 20110166082
    Abstract: A method and compound for treating skeletal muscle mass deficiency in a human subject are disclosed. The composition is an oligomer of morpholino subunits and phosphorus-containing intersubunit linkages joining a morpholino nitrogen of one subunit to a 5? exocyclic carbon of an adjacent subunit, contains between 10-40 nucleotide bases, has a base sequence effective to hybridize to an expression-sensitive region of processed or preprocessed human myostatin RNA transcript, identified, in its processed form, by SEQ ID NO:6, and is capable of uptake by target muscle cells in the subject. In practicing the method, the compound is administered in an amount and at a dosage schedule to produce an overall reduction in the level of serum myostatin measured in the patient, and preferably to bring the myostatin level within the a range determined for normal, healthy individuals.
    Type: Application
    Filed: January 3, 2011
    Publication date: July 7, 2011
    Applicant: AVI BioPharma, Inc.
    Inventors: Patrick L. Iversen, Dwight D. Weller, Alan P. Timmins
  • Publication number: 20110130395
    Abstract: 2-Morpholin-4-yl-9H-purine and 5-Morpholin-4-yl-3H-[1,2,3]triazolo[4,5-d]pyrimidine derivatives, especially those substituted by 6-heteroaryl, are unexpected PI3 kinase isoform selective inhibitors with good drug properties and are useful in treating disorders related to abnormal PI3K activities such as cancer, immune disorders, cardiovascular disease, viral infection, inflammation, metabolism/endocrine disorders and neurological disorders.
    Type: Application
    Filed: July 7, 2009
    Publication date: June 2, 2011
    Inventors: Congxin Liang, Zhigang Li
  • Patent number: 7919490
    Abstract: The present invention provides novel purinones and purines useful for the prevention and treatment of autoimmune diseases, inflammatory disease, mast cell mediated disease and transplant rejection.
    Type: Grant
    Filed: October 4, 2007
    Date of Patent: April 5, 2011
    Assignee: Wyeth LLC
    Inventors: Irina Neagu, David Diller, Celia Kingsbury, Adolph C. Bohnstedt, Michael J. Ohlmeyer, Vidyadhar Paradkar, Nasrin Ansari
  • Patent number: 7902187
    Abstract: The present invention provides novel purinones and purines useful for the prevention and treatment of autoimmune diseases, inflammatory disease, mast cell mediated disease and transplant rejection.
    Type: Grant
    Filed: August 22, 2008
    Date of Patent: March 8, 2011
    Assignee: Wyeth LLC
    Inventors: Irina Neagu, David Diller, Celia Kingsbury, Adolph C. Bohnstedt, Michael J. Ohlmeyer, Vidyadhar Paradkar, Nasrin Ansari
  • Publication number: 20100331302
    Abstract: Compounds are provided that act as potent antagonists of the CCR9 receptor. Animal testing demonstrates that these compounds are useful for treating inflammation, a hallmark disease for CCR9. The compounds are generally aryl sulfonamide derivatives and are useful in pharmaceutical compositions, methods for the treatment of CCR9-mediated diseases, and as controls in assays for the identification of CCR9 antagonists.
    Type: Application
    Filed: July 8, 2010
    Publication date: December 30, 2010
    Applicant: Chemocentryx, Inc.
    Inventors: Trevor T. Charvat, Cheng Hu, Anita Melikian, Aaron Novack, Andrew M.K. Pennell, Edward J. Sullivan, William D. Thomas, Solomon Ungashe, Penglie Zhang, Jay Powers, Sreenivas Punna
  • Publication number: 20100305096
    Abstract: Formula I (Ia and Ib) compounds wherein (i) X1 is N and X2 is S, (ii) X1 is CR7 and X2 is S, (iii) X1 is N and X2 is NR2, or (iv) X1 is CR7 and X2 is O, including stereoisomers, tautomers, metabolites and pharmaceutically acceptable salts thereof, are useful for inhibiting the delta isoform of PI3K, and for treating disorders mediated by lipid kinases such as inflammation, immunological, and cancer. Methods of using compounds of Formula I for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed.
    Type: Application
    Filed: May 26, 2010
    Publication date: December 2, 2010
    Inventors: Georgette Castanedo, Bryan Chan, David Goldstein, Rama Kondru, Matthew Lucas, Wylie Palmer, Stephen Price, Brian Safina, Pascal Pierre Alexandre Savy, Eileen Mary Seward, Daniel P. Sutherlin, Zachary K. Sweeney
  • Publication number: 20100298557
    Abstract: Disclosed is a novel compound having Syk and/or Abl inhibitory activities, which is useful for prevention/treatment of allergic diseases, autoimmune diseases, arthritides and cancers. Specifically disclosed is a pyrazolopyrimidine compound represented by the formula [I] or [III] below, a tautomer thereof, a stereoisomer thereof, a pharmaceutically acceptable salt thereof, or a solvent of any of them.
    Type: Application
    Filed: December 28, 2007
    Publication date: November 25, 2010
    Applicant: Taisho Pharmaceutical Co., Ltd
    Inventors: Makoto Yagi, Hiroki Umemiya, Hajime Asanuma, Yusuke Oka, Rie Nishikawa, Keisi Hayashi, Takumi Okada, Takanori Shimizu, Shigetada Sasako
  • Publication number: 20100204307
    Abstract: The invention relates to a double-stranded ribonucleic acid (dsRNA) for inhibiting the expression of the HAMP gene (HAMP gene), comprising an antisense strand having a nucleotide sequence which is less that 30 nucleotides in length, generally 19-25 nucleotides in length, and which is substantially complementary to at least a part of the HAMP gene. The invention also relates to a pharmaceutical composition comprising the dsRNA together with a pharmaceutically acceptable carrier; methods for treating diseases caused by HAMP gene expression and the expression of the HAMP gene using the pharmaceutical composition.
    Type: Application
    Filed: April 9, 2010
    Publication date: August 12, 2010
    Inventors: Tomoko Nakayama, Anke Geick, Pamela Tan, Herbert Y. Lin
  • Patent number: 7495014
    Abstract: The present invention relates to compounds which inhibit bacterial gyrase and/or Topo IV and pharmaceutically acceptable compositions comprising said compounds. These compounds, and compositions thereof, are useful in treating bacterial infection. Accordingly, the present invention also relates to methods for treating bacterial infections in mammals.
    Type: Grant
    Filed: January 29, 2004
    Date of Patent: February 24, 2009
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: Paul S. Charifson, David D. Deininger, Anne-Laure Grillot, Yusheng Liao, Steven M. Ronkin, Dean Stamos, Emanuele Perola, Tiensheng Wang, Arnaud LeTiran, Joseph Drumm
  • Publication number: 20080300244
    Abstract: The present invention provides compounds of formula wherein R1, Y1, X1, Z1, X2, Y2, A, n and R2 are as defined in the specification, processes for their preparation, pharmaceutical compositions containing them and their use in therapy.
    Type: Application
    Filed: December 13, 2007
    Publication date: December 4, 2008
    Applicant: AstraZeneca AB
    Inventors: Roger Victor BONNERT, Thomas McInally, Tobias Mochel, Stephen Thom
  • Patent number: 7371750
    Abstract: The invention provides a novel class of compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with abnormal or deregulated kinase activity, particularly diseases or disorders that involve abnormal activation of the Abl, BCR-Abl, Bmx, c-Raf, Csk, Fes, FGFR, Flt3, Ikk, IR, JNK, Lck, Mkk, PKC, PKD, Rsk, SAPK, Syk, Trk, BTK, Src, EGFR, IGF, Mek, Ros and Tie2 kinases.
    Type: Grant
    Filed: July 29, 2004
    Date of Patent: May 13, 2008
    Assignee: IRM LLC
    Inventors: Taebo Sim, Hyun Soo Lee, Pingda Ren, Qiang Ding, Guobao Zhang, Yi Liu, Xia Wang, Tetsuo Uno, Bing Li, Lintong Li, Nathanael Schiander Gray, Shuli You
  • Patent number: 7259155
    Abstract: The present invention provides a phosphonic acid diester compound represented by General Formula wherein R1, R2, R3 and R4 are the same or different, and represent hydrogen, halogen, lower alkyl or lower alkoxy; R5 is phenyl having on the phenyl ring 1–3 substituents selected from the group consisting of lower alkyl, halogen-substituted lower alkyl, lower alkoxy, halogen-substituted lower alkoxy, phenoxy, benzyloxy, hydroxyl, halogen, nitro, lower alkylthio, di(lower alkyl)amino, lower alkanolyamino, pyrrolidinyl and phenyl, or the like, provided that R5 is not mono(lower alkoxy)pheny; and R6 is lower alkyl; and an ACAT-1 inhibitor containing the compound as an active ingredient.
    Type: Grant
    Filed: May 5, 2004
    Date of Patent: August 21, 2007
    Assignee: Otsuka Pharmaceutical Factory, Inc.
    Inventors: Yasuhiro Sakai, Kazuyoshi Miyata, Takahiro Tomoyasu, Akiyoshi Kuroda, Yasuhide Inoue, Akifumi Hagi, Shinya Miki, Norihiro Yoshinaga, Masako Doi, Yoshihiko Tsuda, Seiichirou Kanou
  • Patent number: 6838238
    Abstract: This invention provides a method for identifying one or more complexes from a library of complexes, wherein said complex or complexes are selected for their ability to perform a preselected or desired function on a target molecule or by having a pre-selected structure, each complex being designated a morphatide, said method comprising: (a) preparing a library of morphatides, comprised of: (i) a scaffolding component selected from the group consisting of nucleic acid, nucleic acid like molecule or nucleic acid analog having one or more regions of randomized sequence; (ii) one or more linker components; and (iii) one or more agent molecules or type of agent molecules, linked to the scaffolding component by one or more type of linker components; and (b)screening the library of morphatides prepared in step (a) by contacting, binding, or associating the morphatides with one or more suitable target molecules upon which a morphatide performs a preselected or desired function or to which a morphatide binds or associa
    Type: Grant
    Filed: April 14, 1997
    Date of Patent: January 4, 2005
    Assignee: Invitrogen Corporation
    Inventor: Jay M. Short
  • Publication number: 20040265802
    Abstract: Novel oligomers are disclosed which have enhanced ability with respect to forming duplexes or triplexes compared with oligomers containing only conventional bases. The oligomers contain the bases 5-(1-propynyl)uracil, 5-(1-propynyl)cytosine or related analogs. The oligomers of the invention are capable of (i) forming triplexes with various target sequences such as virus or oncogene sequences by coupling into the major groove of a target DNA duplex at physiological pH or (ii) forming duplexes by binding to single-stranded DNA or to RNA encoded by target genes. The oligomers of the invention can be incorporated into pharmaceutically acceptable carriers and can be constructed to have any desired sequence, provided the sequence normally includes one or more bases that is replaced with the analogs of the invention.
    Type: Application
    Filed: November 14, 2002
    Publication date: December 30, 2004
    Inventors: Brian Froehler, Rick Wagner, Mark Matteucci, Robert J. Jones, Arnold J. Gutierrez, Jeff Pudlo
  • Publication number: 20040241683
    Abstract: The invention provides methods and materials related to modulating angiogenesis in an animal. The invention provides polynucleotides and modified polynucleotides such as morpholino-modified polynucleotides for modulating angiogenesis, as well as cells and embryos containing these polynucleotides. The invention also provides methods for identifying HSST- and angiogenesis-modulating agents.
    Type: Application
    Filed: June 14, 2004
    Publication date: December 2, 2004
    Inventors: Stephen C Ekker, Aidas Nasevicius, Eleanor Y Chen
  • Publication number: 20040137485
    Abstract: The invention relates to compositions comprising oligomers antisense to bacterial 16S or 23S rRNA and capable of selectively modulating the biological activity thereof, and methods for their use. More particularly, the invention relates to antisense oligomers directed to 16S or 23S rRNA found in one or more particular bacteria, or generally conserved among bacteria in general, and to pharmaceutical compositions and methods of treatment comprising the same.
    Type: Application
    Filed: November 21, 2003
    Publication date: July 15, 2004
    Applicant: AVI BioPharma, Inc.
    Inventor: Patrick L. Iversen
  • Patent number: 6730676
    Abstract: A class of pyrazino[2,3-d]pyridazine derivatives, possessing an optionally substituted cycloalkyl, phenyl or heteroaryl substituent at the 5-position, a substituted alkoxy moiety at the 3-position, and a range of substituents at the 2-position, are selective ligands for GABAA receptors, in particular having high affinity for the &agr;2 and/or &agr;3 and/or &agr;5 subunit thereof, and are accordingly of benefit in the treatment and/or prevention of adverse conditions of the central nervous system, including anxiety, convulsions and cognitive disorders.
    Type: Grant
    Filed: June 18, 2002
    Date of Patent: May 4, 2004
    Assignee: Merck Sharp & Dohme Ltd.
    Inventors: Wesley Peter Blackaby, Richard Thomas Lewis, Leslie Joseph Street
  • Patent number: 6730681
    Abstract: A class of substituted or 6,7-ring fused [1, 2, 3]triazolo[1,5-&agr;]-pyrimidine derivatives, possessing an optionally substituted cycloalkyl, phenyl or heteroaryl substituent at the 3-position and an amino moiety at the 5-position, are selective ligands for GABAA receptors, in particular having high affinity for the &agr;2 and/or &agr;3 subunit thereof, and are accordingly of benefit in the treatment and/or prevention of disorders of the central nervous system, including anxiety and convulsions.
    Type: Grant
    Filed: June 14, 2002
    Date of Patent: May 4, 2004
    Assignee: Merck Sharp & Dohme Ltd.
    Inventors: Mark Stuart Chambers, Ian James Collins, Simon Charles Goodacre, David James Hallett, Philip Jones, Linda Elizabeth Keown, Robert James Maxey, Leslie Joseph Street
  • Publication number: 20030224353
    Abstract: The invention provides antisense antiviral compounds and methods of their use in inhibition of growth of viruses of the picornavirus, calicivirus, togavirus, coronavirus, and flavivirus families, as in treatment of a viral infection. The antisense antiviral compounds are substantially uncharged oligomers having a targeting base sequence that is substantially complementary to a viral target sequence which spans the AUG start site of the first open reading frame of the viral genome.
    Type: Application
    Filed: April 24, 2003
    Publication date: December 4, 2003
    Inventors: David A. Stein, Douglas E. Skilling, Patrick L. Iversen, Alvin W. Smith