Plural Nitrogens In The Heterocyclic Ring Patents (Class 540/545)
  • Patent number: 10751429
    Abstract: The present disclosure relates to a composition of albumin microbubbles to which are bound one or more moieties that exhibit a binding preference for the albumin microbubbles relative to free, native HSA. Production of the albumin microbubble composition and use of the albumin microbubble composition in ultrasound mediated delivery of therapeutic or diagnostic agents is also discussed.
    Type: Grant
    Filed: August 13, 2018
    Date of Patent: August 25, 2020
    Assignee: GENERAL ELECTRIC COMPANY
    Inventors: Matthew David Butts, Jason William Castle, Andrew Soliz Torres, Jeannette Christine Roberts, Binil Itty Ipe Kandapallil
  • Publication number: 20150065485
    Abstract: This invention provides compounds having antiviral activities especially inhibiting activity for influenza virus, more preferably provides substituted 3-hydroxy-4-pyridone derivatives having cap-dependent endonuclease inhibitory activity.
    Type: Application
    Filed: November 7, 2014
    Publication date: March 5, 2015
    Inventors: Toshiyuki Akiyama, Kenji Takaya, Makoto Kawai, Yoshiyuki Taoda, Minako Mikamiyama, Kenji Morimoto, Chika Kageyama, Kenji Tomita, Hidenori Mikamiyama, Naoyuki Suzuki
  • Publication number: 20140350243
    Abstract: The present invention relates to compounds of the formula (1) which are suitable for use in electronic devices, in particular organic electroluminescent devices.
    Type: Application
    Filed: August 7, 2014
    Publication date: November 27, 2014
    Applicant: Merch Patent GmbH
    Inventors: Amir Hossain Parham, Christof Pflumm, Teresa Mujica-Fernaud
  • Publication number: 20140323412
    Abstract: Provided herein are methods of treating or ameliorating hypercholemia or a cholestatic liver disease by administering to an individual in need thereof a therapeutically effective amount of an Apical Sodium-dependent Bile Acid Transporter Inhibitor (ASBTI) or a pharmaceutically acceptable salt thereof. Also provided are methods for treating or ameliorating a liver disease, decreasing the levels of serum bile acids or hepatic bile acids, treating or ameliorating pruritis, reducing liver enzymes, or reducing bilirubin comprising administering to an individual in need thereof a therapeutically effective amount of ASBTI or a pharmaceutically acceptable salt thereof.
    Type: Application
    Filed: October 26, 2012
    Publication date: October 30, 2014
    Inventors: Bronislava Gedulin, Michael Grey, Niall O'Donnell
  • Publication number: 20140302988
    Abstract: The invention relates to novel compounds of the formula (I) in which X, Y and CKE have the meanings given above, to a plurality of processes and intermediates for their preparation, and to their use as pesticides and/or herbicides. The invention also relates to selective herbicidal compositions comprising, firstly, the 1,2,4-triazolyl-substituted ketoenols and, secondly, a crop plant compatibility-improving compound. The present invention furthermore relates to the boosting of the action of crop protection compositions comprising, in particular, 1,2,4-triazolyl-substituted ketoenols, through the addition of ammonium salts or phosphonium salts and optionally penetrants, to the corresponding compositions, to processes for producing them and to their application in crop protection as insecticides and/or acaricides and/or for preventing unwanted plant growth.
    Type: Application
    Filed: August 10, 2012
    Publication date: October 9, 2014
    Applicant: Bayer Intellectual Property GMBH
    Inventors: Wolfgang Gienckle, Stefan Lehr, Reiner Fischer, David Stephen Lindell, Isolde Haeuser-Hahn, Ines Heinemann, Elmar Gatzweiler, Christopher Hugh Rosinger, Angela Becker, Arnd Voerste, Ulrich D.I. Goergens
  • Publication number: 20140275032
    Abstract: Compounds of the formula I: or pharmaceutically acceptable salts thereof, wherein m, n, p, q, r, A, X1, X2, X3, X4, X5, X6, Y, Z, G, R1a, R2a, R1b, R2b, R3, R4, R5 and R6 are as defined herein. Also disclosed are methods of making the compounds and using the compounds for treatment of inflammatory diseases such as arthritis.
    Type: Application
    Filed: March 14, 2014
    Publication date: September 18, 2014
    Applicant: Genentech, Inc.
    Inventors: Benjamin Fauber, Olivier Rene, Monique Bodil van Niel, Stuart Ward
  • Patent number: 8809318
    Abstract: In its many embodiments, the present invention provides a novel class of heterocyclic compounds of the formula: as modulators of gamma secretase, methods of preparing such compounds, pharmaceutical compositions containing one or more such compounds, methods of preparing pharmaceutical formulations comprising one or more such compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more disease associated with the central nervous system using such compounds or pharmaceutical compostions.
    Type: Grant
    Filed: November 11, 2009
    Date of Patent: August 19, 2014
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Zhaoning Zhu, William J. Greenlee, Hongmei Li, Monica L. Vicarel, Jun Qin, Pawan Kumar Dhondi, Xianhai Huang, Anandan Palani, Xiaoxiang Liu, Zhong-Yue Sun, Hubert B. Josien, Ruo Xu, David James Cole, Duane A. Burnett, Chad E. Bennett, Troy McCracken, Malcolm MacCoss
  • Patent number: 8785625
    Abstract: The invention provides a novel oxazolidinone derivative represented by the formula (I): wherein Ring A, X1, Ring B and R1 are as described in the description, and an antibacterial agent containing the same.
    Type: Grant
    Filed: February 14, 2012
    Date of Patent: July 22, 2014
    Assignees: Research Foundation Itsuu Laboratory, Shionogi & Co., Ltd.
    Inventors: Hideyuki Suzuki, Shoji Hizatate, Iwao Utsunomiya, Koichi Shudo
  • Patent number: 8771682
    Abstract: The present invention relates generally to methods and compositions for reducing Interleukin-4 or Interleukin-13 signaling, in particular to treat asthma and atopic dermatitis. The inventors have found that Rac/PAK mediated endocytosis of the ligand bound type I (IL-4R with the chains IL-4Ra and IL-2-Rg) and/or type II receptor (IL-13R with the chains IL-4Ra and IL-13Ra1) is needed for the IL-4 and/or IL-13 mediated activation of downstream signalling events including phosphorylation of Stat family transcrition factors. These discoveries enable new methods of screening compounds that modulate Interleukin-4 and Interleukin-13 signalling, as well as new methods for treating conditions characterized by increased Interleukin-4 and Interleukin-13 levels. These conditions include inflammatory conditions, asthma bronchiale, atopic dermatitis, allergies, atopic syndromes, allergic rhinitis, and th2-induced conditions.
    Type: Grant
    Filed: April 26, 2012
    Date of Patent: July 8, 2014
    Assignee: Technische Universtität Dresden
    Inventors: Christian Bökel, Thomas Weidemann
  • Publication number: 20140179677
    Abstract: A novel therapeutic agent for ectopic pregnancy having a therapeutic effect for ectopic pregnancy, especially unruptured ectopic pregnancy, and a novel method of screening a therapeutic agent for ectopic pregnancy are disclosed. The therapeutic agent for ectopic pregnancy contains as an effective ingredient a suppressor of brain-derived neurotrophic factor (BDNF) and/or of brain-derived neurotrophic factor receptor (TrkB). The method of screening a therapeutic agent for ectopic pregnancy includes measuring the kinase activity of TrkB in the presence of a test substance and the kinase activity of TrkB in the absence of the test substance; and selecting the test substance which decreases the kinase activity of TrkB.
    Type: Application
    Filed: December 28, 2011
    Publication date: June 26, 2014
    Applicant: AKITA UNIVERSITY
    Inventor: Kazuhiro Kawamura
  • Patent number: 8729065
    Abstract: Described are crystalline forms of the pharmaceutical compound “[9S-(9?,10?,12?)]-5,16-Bis[(ethylthio)methyl]-2,3,9,10,11,12-hexahydro-10-hydroxy-9-methyl-1-oxo-9,12-epoxy-1H-diindolo[1,2,3-fg:3?,2?,1?-kl]pyrrolo[3,4-i][1,6]benzodiazocine-10-carboxylic acid methyl ester”, as well as methods for their use and preparation.
    Type: Grant
    Filed: January 3, 2011
    Date of Patent: May 20, 2014
    Assignee: Cephalon, Inc.
    Inventors: Michael Harold Rock, Heidi Lopez De Diego, Kim Lasse Christensen, Ole Nielsen, Anders Buur, Mark Howells
  • Patent number: 8722663
    Abstract: The present invention provides a novel compound having an excellent antitumor effect. The compound of the present invention is represented by the following general formula (1) wherein R1 and R2 are aryl or the like; A is lower alkylene; Ring X is optionally substituted arylene; E is bond or lower alkenylene; Ring Y is optionally substituted heterocycloalkylene containing one or more nitrogen atoms, one of which is attached to the adjacent carbonyl group; G is —NH-G2-, —N(lower alkyl)-G2-, —NH—CH2-G2-, —N(lower alkyl)-CH2-G2- or —CH2-G2-, [wherein G2 binds to R2, G2-R2 is bond-R2, phenylene-G3-R2, phenylene-G4-O—R2, phenylene-G5-NH—R2, phenylene-G6-N(lower alkyl)-R2 or quinolinediyl-O—R2, the phenylene of said phenylene-containing groups being optionally substituted with one or more substituents; G3-R2 is —O-lower alkylene-R2 or the like; G4-O— is lower alkylene-O— or the like; G5 is lower alkylene; G6 is lower alkylene].
    Type: Grant
    Filed: January 28, 2011
    Date of Patent: May 13, 2014
    Assignee: Otsuka Pharmaceutical Co., Ltd.
    Inventors: Hideki Takasu, Shigekazu Fujita, Shinya Ohtsuka, Toshiyuki Hirose, Yosuke Sato, Satoshi Yamada, Keisuke Miyajima, Koji Sakai, Yutaka Kojima, Kazuo Sekiguchi, Yasuo Yanagihara, Takashi Suzuki, Hideo Tanaka, Kazuhisa Sugiyama, Mitsuhiro Okuno, Takumi Sumida
  • Patent number: 8710216
    Abstract: The invention relates to a new crystalline form II of N-benzoyl-staurosporine; compositions containing the same; processes for the preparation thereof; and the use of crystalline form II of of N-benzoyl-staurosporine in diagnostic methods or therapeutic treatment of warm-blooded animals, especially humans. The invention relates to the amorphous forms of N-benzoyl-staurosporine; compositions containing the same; processes for the preparation thereof; and the use of amorphous N-benzoyl-staurosporine in diagnostic methods or therapeutic treatment of warm-blooded animals, especially humans.
    Type: Grant
    Filed: May 15, 2012
    Date of Patent: April 29, 2014
    Assignee: Novartis AG
    Inventors: Pascale Hoehn, Bernd Koch, Michael Mutz
  • Patent number: 8685960
    Abstract: The invention provides compounds of the general formula (I) which are inhibitors of the human aldosterone synthase, and also pharmaceutical compositions containing these compounds, and the use of these compounds and other heteroaryl substituted quinolinone derivatives for the treatment of hyperaldosteronism and/or disorders or diseases that are mediated by 11 ?-hydroxylase (CYP11 B1).
    Type: Grant
    Filed: May 5, 2009
    Date of Patent: April 1, 2014
    Assignee: Elexopharm GmbH
    Inventors: Rolf W. Hartmann, Ralf Heim, Simon Lucas
  • Publication number: 20140066488
    Abstract: Proteases such as memapsin 2 are important enzymes, playing roles in a variety of diseases including Alzheimer's Disease. The inventors have developed inhibitors of memapsin 2 and methods of use therefore in the treatment of disease.
    Type: Application
    Filed: August 28, 2013
    Publication date: March 6, 2014
    Applicants: Purdue Research Foundation, Oklahoma Medical Research Foundation
    Inventors: Jordan Tang, Venkateswararao Kalapala, Arun K. Ghosh
  • Publication number: 20140024636
    Abstract: Provided is a sulfamide derivative having an adamantyl group represented by the following Formula 1, or a pharmaceutically acceptable salt thereof. The sulfamide derivative suppresses the activity of 11?-hydroxysteroid dehydrogenase type 1 (11?-HSD1), and is useful in the treatment of various diseases that are mediated by 11?-HSD1.
    Type: Application
    Filed: March 30, 2012
    Publication date: January 23, 2014
    Applicant: KOREA RESEARCH INSTITUTE OF CHEMICAL TECHNOLOGY
    Inventors: Ki Young Kim, Jin Hee Ahn, Seung Kyu Kang, Sang Dal Rhee, Myung Ae Bae, Sung Hoon Ahn, Hee Youn Kim, Won Hoon Jung, Nam Sook Kang
  • Publication number: 20130310340
    Abstract: A method for treating muscular deterioration is disclosed. Also disclosed are embodiments of a compound, and compositions comprising the compound, for inhibiting muscular deterioriation, including atrophy, dystrophy, and cachexia, such as may result from ventilation.
    Type: Application
    Filed: May 15, 2013
    Publication date: November 21, 2013
    Applicant: Rigel Pharmaceuticals, Inc.
    Inventors: Donald G. Payan, Esteban Masuda, Todd Kinsella
  • Patent number: 8575146
    Abstract: This application relates to the use of staurosporines derivatives for the curative, palliative or prophylactic treatment of allergic rhinitis, allergic dermatitis, drug allergy or food allergy, angioedema, urticaria, sudden infant death syndrome, bronchopulmonary aspergillosis, multiple sclerosis, or mastocytosis; and to a method of treatment of warm-blooded animals in which a therapeutically effective dose of a compound of a Staurosporine Derivative is administered to a warm-blooded animal suffering from one of the diseases or conditions mentioned above.
    Type: Grant
    Filed: June 17, 2004
    Date of Patent: November 5, 2013
    Assignee: Novartis AG
    Inventor: Steven Coutre
  • Patent number: 8541404
    Abstract: The invention provides compounds of the general formula (I) which are inhibitors of the human aldosterone synthase, and also pharmaceutical compositions containing these compounds, and a method of treating of hyperaldosteronism and/or disorders or diseases that are mediated by 11?-hydroxylase (CYP11B1) with these compounds.
    Type: Grant
    Filed: November 3, 2010
    Date of Patent: September 24, 2013
    Assignee: ElexoPharm GmbH
    Inventors: Rolf W. Hartmann, Ralf Heim, Simon Lucas
  • Patent number: 8530646
    Abstract: The present invention provides a novel oxazolidinone derivative of the formula (I): wherein Rings A and B are defined as in the specification; X1is a single bond, or a heteroatom-containing group selected from the group consisting of —O—, —S—, —NR2—, —CO—, —CS—, —CONR3—, —NR4CO—, —SONR5—, and NR6SO2—, wherein R2, R3, R4, R5, and R6 are independently hydrogen or lower alkyl, or lower alkylene or lower alkenylene each optionally interrupted by said heteroatom containing group; and R1 is hydrogen, or an organic residue which is able to bind to the 5-position of the oxazolidinone ring in oxazolidinone antimicrobial agents, pharmaceutically acceptable salts and solvates thereof which are useful as an antibacterial agent.
    Type: Grant
    Filed: October 1, 2008
    Date of Patent: September 10, 2013
    Assignees: Research Foundation Itsuu Laboratory, Shionogi & Co., Ltd.
    Inventors: Hideyuki Suzuki, Iwao Utsunomiya, Koichi Shudo, Tsutomu Iwaki, Tatsuro Yasukata
  • Publication number: 20130225511
    Abstract: The present invention regards specific IBAT inhibitors useful in the prophylaxis and/or treatment of a liver disease. It also relates to compositions comprising these IBAT inhibitors, a method for treatment of the disorders and a kit comprising the substances or the compositions.
    Type: Application
    Filed: November 8, 2011
    Publication date: August 29, 2013
    Inventors: Per-Göran Gillberg, Hans Graffner, Ingemar Starke
  • Patent number: 8445479
    Abstract: The present invention relates to the use of staurosporines derivatives for the preparation of a drug for the treatment of diseases involving deregulated FLT3 receptor tyrosine kinase activity, especially for the curative and/or prophylactic treatment of leukemias and myelodysplastic syndromes, and to a method of treating diseases involving deregulated FLT3 receptor tyrosine kinase activity.
    Type: Grant
    Filed: June 15, 2012
    Date of Patent: May 21, 2013
    Assignees: Novartis AG, Dana-Farber-Cancer Institute Inc.
    Inventors: James Douglas Griffin, Paul William Manley
  • Publication number: 20130122064
    Abstract: The present invention relates to ophthalmic depot formulations comprising an active agent, e.g. embedded in a pharmacologically acceptable biocompatible polymer or a lipid encapsulating agent, e.g. for periocular or subconjunctival administration.
    Type: Application
    Filed: January 7, 2013
    Publication date: May 16, 2013
    Applicant: NOVARTIS AG
    Inventor: NOVARTIS AG
  • Publication number: 20130084275
    Abstract: The present invention relates generally to methods and compositions for reducing Interleukin-4 or Interleukin-13 signaling, in particular to treat asthma and atopic dermatitis. The inventors have found that Rac/PAK mediated endocytosis of the ligand bound type I (IL-4R with the chains IL-4Ra and IL-2-Rg) and/or type II receptor (IL-13R with the chains IL-4Ra and IL-13Ra1) is needed for the IL-4 and/or IL-13 mediated activation of downstream signalling events including phosphorylation of Stat family transcrition factors. These discoveries enable new methods of screening compounds that modulate Interleukin-4 and Interleukin-13 signalling, as well as new methods for treating conditions characterized by increased Interleukin-4 and Interleukin-13 levels. These conditions include inflammatory conditions, asthma bronchiale, atopic dermatitis, allergies, atopic syndromes, allergic rhinitis, and th2-induced conditions.
    Type: Application
    Filed: April 26, 2012
    Publication date: April 4, 2013
    Applicant: Technische Universitat Dresden
    Inventors: Christian Bôkel, Thomas Weidemann
  • Publication number: 20130052205
    Abstract: The present invention relates to FLT3 receptor antagonists or inhibitors of FLT3 receptor gene expression for the treatment or the prevention of pain disorders.
    Type: Application
    Filed: January 5, 2011
    Publication date: February 28, 2013
    Inventor: Jean Valmier
  • Publication number: 20130040935
    Abstract: The invention relates to 5?-biphenyl-substituted cyclic ketoenols for therapeutic purposes, to pharmaceutical compositions and to their use in therapy, in particular for the prophylaxis and therapy of tumour disorders.
    Type: Application
    Filed: February 8, 2011
    Publication date: February 14, 2013
    Applicant: BAYER INTELLECTUAL PROPERTY GMBH
    Inventors: Ningshu Liu, Kai Thede, Philip Lienau, Arne Scholz, Christoph-Stephan Hilger, Ulf Bömer, Maher Najjar, Knut Eis, Reiner Fischer, Wahed Ahmed Moradi
  • Publication number: 20130012700
    Abstract: The present invention relates to compounds of the formula (1) which are suitable for use in electronic devices, in particular organic electroluminescent devices.
    Type: Application
    Filed: February 25, 2011
    Publication date: January 10, 2013
    Applicant: Merck Patent GmbH
    Inventors: Amir Hossain Parham, Christof Pflumm, Teresa Mujica-Fernaud
  • Publication number: 20120329779
    Abstract: The present invention relates to a method of treating a warm-blooded animal, especially a human, having Mixed Lineage Leukemia (MLL rearranged ALL) comprising administering to said animal a therapeutically effective amount of a staurosporine derivative, especially PKC412 or a pharmaceutically acceptable salt thereof, alone or in combination with further therapeutic measures, for example, those defined herein; to the use of a staurosporine derivative for the preparation of a medicament for the treatment of MLL rearranged ALL; and to a commercial package comprising a staurosporine derivative together with instructions for its use in the treatment of MLL rearranged ALL.
    Type: Application
    Filed: September 7, 2012
    Publication date: December 27, 2012
    Inventors: James Douglas Griffin, Doriano Fabbro
  • Publication number: 20120322789
    Abstract: The invention relates to a new crystalline form II of N-benzoyl-staurosporine; compositions containing the same; processes for the preparation thereof; and the use of crystalline form II of of N-benzoyl-staurosporine in diagnostic methods or therapeutic treatment of warm-blooded animals, especially humans. The invention relates to the amorphous forms of N-benzoyl-staurosporine; compositions containing the same; processes for the preparation thereof; and the use of amorphous N-benzoyl-staurosporine in diagnostic methods or therapeutic treatment of warm-blooded animals, especially humans.
    Type: Application
    Filed: May 15, 2012
    Publication date: December 20, 2012
    Inventors: Pascale HOEHN, Bernd KOCH, Michael MUTZ
  • Patent number: 8309540
    Abstract: The present invention relates to macrocyclic compounds of formula (I) that are useful as inhibitors of the hepatitis C virus (HCV) NS3 protease, their synthesis, and their use for treating or preventing HCV infections.
    Type: Grant
    Filed: October 22, 2007
    Date of Patent: November 13, 2012
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Nigel J. Liverton, Joseph P. Vacca, John A. McCauley, Joseph J. Romano, Michael T. Rudd
  • Publication number: 20120283242
    Abstract: The present invention provides a novel compound having an excellent antitumor effect. The compound of the present invention is represented by the following general formula (1) wherein R1 and R2 are aryl or the like; A is lower alkylene; Ring X is optionally substituted arylene; E is bond or lower alkenylene; Ring Y is optionally substituted heterocycloalkylene containing one or more nitrogen atoms, one of which is attached to the adjacent carbonyl group; G is —NH-G2-, —N(lower alkyl)-G2-, —NH—CH2-G2-, —N(lower alkyl)-CH2-G2- or —CH2-G2-, [wherein G2 binds to R2, G2-R2 is bond-R2, phenylene-G3-R2, phenylene-G4-O—R2, phenylene-G5-NH—R2, phenylene-G6-N(lower alkyl)-R2 or quinolinediyl-O—R2, the phenylene of said phenylene-containing groups being optionally substituted with one or more substituents; G3-R2 is —O-lower alkylene-R2 or the like; G4-O— is lower alkylene-O— or the like; G5 is lower alkylene; G6 is lower alkylene].
    Type: Application
    Filed: January 28, 2011
    Publication date: November 8, 2012
    Inventors: Hideki Takasu, Shigekazu Fujita, Shinya Ohtsuka, Toshiyuki Hirose, Yosuke Sato, Satoshi Yamada, Keisuke Miyajima, Koji Sakai, Yutaka Kojima, Kazuo Sekiguchi, Yasuo Yanagihara, Takashi Suzuki, Hideo Tanaka, Kazuhisa Sugiyama, Mitsuhiro Okuno, Takumi Sumida
  • Publication number: 20120269894
    Abstract: The present invention relates to ophthalmic depot formulations comprising an active agent, e.g. embedded in a pharmacologically acceptable biocompatible polymer or a lipid encapsulating agent, e.g. for periocular or subconjunctival administration.
    Type: Application
    Filed: June 14, 2012
    Publication date: October 25, 2012
    Inventors: Marklus AHLHEIM, Michael AUSBORN, David BODMER, Christian SCHOCH
  • Publication number: 20120252784
    Abstract: Novel 2,3,4-benzothiadiazepines-2,2-dioxides and processes for the preparation thereof are disclosed. The compounds influence the central nervous system and may be used to treat or prevent Alzheimer's disease, Parkinson's disease or Huntington's disease, senile dementia not of the Alzheimer's type, vascular dementia, post-stroke dementia, Korsakoff's syndrome, Down's syndrome, schizophrenia, panic disorder, post-traumatic stress disorder, anxiety or depression.
    Type: Application
    Filed: March 13, 2012
    Publication date: October 4, 2012
    Inventors: Jozsef FETTER, Ferenc BERTHA, Balazs MOLNAR, Gyula SIMIG, Jozsef BARKOCZY, Balazs VOLK, Gyoergy LEVAY, Istvan GACSALYI, Gabor GIGLER, Hajnalka KOMPAGNE, Bernadett MARKO, Katalin NAGY, Peter KIRICSI, Laszlo Gabor HARSING, Gabor SZENASI
  • Publication number: 20120245160
    Abstract: The present invention relates to a crystalline form III and a crystalline form IV of N-benzoyl staurosporine. N-benzoyl staurosporine is also known as Midostaurin or PKC412.
    Type: Application
    Filed: November 29, 2010
    Publication date: September 27, 2012
    Inventor: Ranjit Thakur
  • Publication number: 20120238546
    Abstract: This invention provides novel compounds that are modulators of gamma secretase. The compounds have the Formula (I): Also disclosed are methods of modulating gamma secretase activity and methods of treating Alzheimer's Disease using the compounds of Formula (I).
    Type: Application
    Filed: June 15, 2010
    Publication date: September 20, 2012
    Inventors: Zhaoning Zhu, Xianhai Huang, Anandan Palani, William J. Greenlee, Robert G. Aslanian
  • Publication number: 20120208997
    Abstract: The invention provides a novel oxazolidinone derivative represented by the formula (I): wherein Ring A, X1, Ring B and R1 are as described in the description, and an antibacterial agent containing the same.
    Type: Application
    Filed: February 14, 2012
    Publication date: August 16, 2012
    Inventors: Hideyuki SUZUKI, Shoji HIZATATE, Iwao UTSUNOMIYA, Koichi SHUDO
  • Patent number: 8236790
    Abstract: Compounds of formula (I): wherein: R1 and R2, which may be the same or different, each represent a hydrogen or halogen atom or an alkyl, alkoxy, alkylthio, acyl, alkoxycarbonyl, carboxy, hydroxy, hydroxyalkyl, cyano, nitro, amino, substituted or unsubstituted aminocarbonyl, aminosulphonyl, alkylsulphonylaminoalkyl, N-hydroxy-carboximidamide or benzyloxy group, R3 represents a hydrogen atom or an alkyl, cycloalkyl or cycloalkylalkyl group, R4 represents a hydrogen atom or a substituted or unsubstituted alkyl group Medicinal products containing the same which are useful in treating or preventing conditions treatable by an AMPA receptor modulator and/or an NMDA receptor antagonist.
    Type: Grant
    Filed: March 19, 2010
    Date of Patent: August 7, 2012
    Assignee: Les Laboratories Servier
    Inventors: Alexis Cordi, Patrice Desos, Pierre Lestage, Laurence Danober
  • Publication number: 20120184734
    Abstract: This invention provides compounds having antiviral activities especially inhibiting activity for influenza virus, more preferably provides substituted 3-hydroxy-4-pyridone derivatives having cap-dependent endonuclease inhibitory activity.
    Type: Application
    Filed: June 14, 2010
    Publication date: July 19, 2012
    Inventors: Toshiyuki Akiyama, Kenji Takaya, Makoto Kawai, Yoshiyuki Taoda, Minako Mikamiyama, Kenji Morimoto, Chika Kageyama, Kenji Tomita, Hidenori Mikamiyama, Naoyuki Suzuki
  • Patent number: 8222244
    Abstract: The present invention relates to the use of staurosporines derivatives for the preparation of a drug for the treatment of diseases involving deregulated FLT3 receptor tyrosine kinase activity, especially for the curative and/or prophylactic treatment of leukemias and myelodysplastic syndromes, and to a method of treating diseases involving deregulated FLT3 receptor tyrosine kinase activity.
    Type: Grant
    Filed: May 17, 2011
    Date of Patent: July 17, 2012
    Assignees: Novartis AG, Dana-Farber Cancer Institute Inc.
    Inventors: James D Griffin, Paul W Manley
  • Publication number: 20120149685
    Abstract: The present invention refers to the use of a specific indolocarbazole compound of general formula (1) or a pharmaceutically-acceptable a salt thereof for the preparation of a pharmaceutical composition for the prevention or treatment of a neurode-generative and/or dementing illness driven by the molecular pathology of microtubule-associate tau such as Alzheimer's disease, frontal lobe dementia, Pick's disease, Parkinson disease with dementia, corticobasal degeneration, argyrophilic grains disease, or supranuclear palsy. A method for treating or preventing such illnesses is also disclosed. Furthermore, methods for the identification of efficacious inhibitors of neurofibrillary degeneration, and methods for the determination of an appropriate dosage of an inhibitor of the PHF-type tau hyperphosphorylation for the treatment of a condition characterized by neurofibrillary pathology are described.
    Type: Application
    Filed: July 19, 2011
    Publication date: June 14, 2012
    Applicant: Tautatis, Inc.
    Inventor: Hanno RODER
  • Patent number: 8198435
    Abstract: The invention relates to a new crystalline form II of N-benzoyl-staurosporine; compositions containing the same; processes for the preparation thereof; and the use of crystalline form II of N-benzoyl-staurosporine in diagnostic methods or therapeutic treatment of warm-blooded animals, especially humans. The invention relates to the amorphous forms of N-benzoyl-staurosporine; compositions containing the same; processes for the preparation thereof; and the use of amorphous N-benzoyl-staurosporine in diagnostic methods or therapeutic treatment of warm-blooded animals, especially humans.
    Type: Grant
    Filed: November 3, 2005
    Date of Patent: June 12, 2012
    Assignee: Novartis AG
    Inventors: Pascale Hoehn, Bernd Koch, Michael Mutz
  • Publication number: 20120129833
    Abstract: The invention relates to 5?-biphenyl-substituted cyclic ketoenols for therapeutic purposes, to pharmaceutical compositions and to their use in therapy, in particular for the prophylaxis and therapy of diabetes, obesity, hyperlipidaemia, fatty livers and of disorders of the cardiovascular system.
    Type: Application
    Filed: August 19, 2011
    Publication date: May 24, 2012
    Applicant: BAYER PHARMA AKTIENGESELLSCHAFT
    Inventors: Ningshu LIU, Kai Thede, Philip Lienau, Arne Scholz, Maher Najjar, Ulf Bomer, Knut Eis, Reiner Fischer
  • Publication number: 20120114588
    Abstract: The present invention regards specific IBAT inhibitors with improved effect in prophylaxis and treatment of metabolic syndrome, obesity, disorders of fatty acid metabolism, glucose utilization disorders, disorders in which insulin resistance is involved, diabetes mellitus, type 1 and type 2 diabetes. It also relates to compositions comprising these IBAT inhibitors, a method for treatment of the disorders and a kit comprising the substances or the compositions.
    Type: Application
    Filed: May 26, 2011
    Publication date: May 10, 2012
    Applicant: ALBIREO AB
    Inventors: Ingemar Starke, Hans Graffner, Per-Göran Gillberg, Ann-Margret Lindqvist, Bo Angelin
  • Patent number: 8119566
    Abstract: The present invention relates to novel 4-biphenyl-substituted pyrazolidine-3,5-dione derivatives of the formula (I) in which A, D, G, W, X, Y and Z are as defined above, to a plurality of processes for the preparation and to their use as pesticides and/or herbicides and/or microbicides. Moreover, the invention relates to selective herbicidal compositions comprising both the 4-biphenyl-substituted pyrazolidine-3,5-dione derivatives of the formula (I) and a crop plant compatibility-improving compound.
    Type: Grant
    Filed: August 2, 2004
    Date of Patent: February 21, 2012
    Assignee: Bayer CropScience AG
    Inventors: Reiner Fischer, Thomas Bretschneider, Ernst Rudolf F. Gesing, Dieter Feucht, Karl-Heinz Kuck, Peter Lösel, Olga Malsam, Christian Arnold, Thomas Auler, Martin Jeffrey Hills, Heinz Kehne
  • Publication number: 20110306593
    Abstract: In its many embodiments, the present invention provides a novel class of heterocyclic compounds of the formula: as modulators of gamma secretase, methods of preparing such compounds, pharmaceutical compositions containing one or more such compounds, methods of preparing pharmaceutical formulations comprising one or more such compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more disease associated with the central nervous system using such compounds or pharmaceutical compostions.
    Type: Application
    Filed: November 11, 2009
    Publication date: December 15, 2011
    Inventors: Zhaoning Zhu, William J. Greenlee, Hongmei Li, Monica L. Vicarel, Jun Qin, Pawan Kumar Dhondi, Xianhai Huang, Anandan Palani, Xiaoxiang Liu, Zhong-Yue Sun, Hubert B. Josien, Ruo Xu, David James Cole, Duane A. Burnett, Chad E. Bennett, Troy McCracken, Malcolm MacCoss
  • Patent number: 8076320
    Abstract: Described are crystalline forms of the pharmaceutical compound “[9S-(9?,10?,12?)]-5,16-Bis[(ethylthio)methyl]-2,3,9,10,11,12-hexahydro-10-hydroxy-9-methyl-1-oxo-9, 12-epoxy-1H-diindolo[1,2,3-fg:3?,2?,1?-kl]pyrrolo[3,4-i][1,6]benzodiazocine-10-carboxylic acid methyl ester”, as well as methods for their use and preparation.
    Type: Grant
    Filed: February 24, 2005
    Date of Patent: December 13, 2011
    Assignee: Cephalon, Inc.
    Inventors: Michael Harold Rock, Heidi Lopez De Diego, Kim Lasse Christensen, Ole Nielsen, Anders Buur, Mark Howells
  • Publication number: 20110294783
    Abstract: The present invention concerns boosting the activity of crop protection materials comprising inhibitors of fatty acid biosynthesis (for example phenyl-substituted cyclic ketoenols) through the addition of ammonium salts and/or phosphonium salts or through the addition of ammonium salts and/or phosphonium salts and penetrants, the corresponding materials, processes for preparing them, and their use in crop protection.
    Type: Application
    Filed: August 10, 2011
    Publication date: December 1, 2011
    Applicant: BAYER CROPSCIENCE AG
    Inventors: Reiner FISCHER, Stefan LEHR, Peter MARCZOK, Udo Reckmann, Christian Arnold, Waltraud Hempel, Erich SANWALD, Rolf Pontzen
  • Publication number: 20110207925
    Abstract: A process for the preparation of [1,4,5]-oxadiazepine derivatives by reaction of 4,5-diacyl-[1,4,5]-oxadiazepines with a base.
    Type: Application
    Filed: May 4, 2011
    Publication date: August 25, 2011
    Applicant: SYNGENTA CROP PROTECTION, INC.
    Inventors: Dominik Faber, Beat Jau
  • Publication number: 20110172206
    Abstract: Compounds, compositions, kits and methods for treating conditions related to neurodegeneration or ocular disease, are disclosed.
    Type: Application
    Filed: August 8, 2009
    Publication date: July 14, 2011
    Applicant: THE JOHNS HOPKINS UNIVERSITY
    Inventors: Donald Jeffrey Zack, Zhiyong Yang, Cynthia Berlinicke, Harry Quigley
  • Patent number: 7973031
    Abstract: The present invention relates to the use of staurosporines derivatives for the preparation of a drug for the treatment of diseases involving deregulated FLT3 receptor tyrosine kinase activity, especially for the curative and/or prophylactic treatment of leukemias and myelodysplastic syndromes, and to a method of treating diseases involving deregulated FLT3 receptor tyrosine kinase activity.
    Type: Grant
    Filed: October 29, 2002
    Date of Patent: July 5, 2011
    Assignees: Novartis AG, Dana-Farber Cancer Institute Inc
    Inventors: James Douglas Griffin, Paul William Manley