Polycyclo Ring System Having The Seven-membered Hetero Ring As One Of The Cyclos Patents (Class 514/212.04)
  • Patent number: 10865188
    Abstract: The present disclosure provides crystalline Compound I and crystalline Compound II, pharmaceutical compositions comprising one of said crystalline compounds suitable for intratympanic administration, and methods for treating otic disorders using the crystalline compounds and the pharmaceutical compositions.
    Type: Grant
    Filed: March 4, 2019
    Date of Patent: December 15, 2020
    Assignee: Pipeline Therapeutics, Inc.
    Inventors: Thomas Jon Seiders, Catherine Yuling Lee, Yiwei Li
  • Patent number: 10301266
    Abstract: The present disclosure provides crystalline Compound I and crystalline Compound II, pharmaceutical compositions comprising one of said crystalline compounds suitable for intratympanic administration, and methods for treating otic disorders using the crystalline compounds and the pharmaceutical compositions.
    Type: Grant
    Filed: April 10, 2018
    Date of Patent: May 28, 2019
    Assignee: Inception 3, Inc.
    Inventors: Thomas Jon Seiders, Catherine Yuling Lee, Yiwei Li
  • Patent number: 9913848
    Abstract: The present invention relates to methods of inducing the self-renewal of stem/progenitor supporting cells, including inducing the stem/progenitor cells to proliferate while maintaining, in the daughter cells, the capacity to differentiate into hair cells. Specifically, the invention relates to methods of using compounds comprising a 1,2,3,4-tetrahydro-[1,4]diazepino[6,7, 1-hi]indole moiety having a Formula I and pharmaceutically acceptable salts thereof.
    Type: Grant
    Filed: March 2, 2017
    Date of Patent: March 13, 2018
    Assignee: Frequency Therapeutics, Inc.
    Inventors: Christopher Loose, Will McLean, Melissa Hill-Drzewi
  • Patent number: 9144543
    Abstract: Biocompatible intraocular implants include an alpha-2 adrenergic receptor agonist and a polymer associated with the alpha-2 adrenergic receptor agonist to facilitate release of the alpha-2 adrenergic receptor agonist into an eye for an extended period of time. The alpha-2 adrenergic receptor agonist may be associated with a biodegradable polymer matrix, such as a matrix of a two biodegradable polymers. The implants may be placed in an eye to prevent the occurrence of one or more ocular conditions, or to reduce one or more symptoms of an ocular condition, such as an ocular neurosensory disorder and the like.
    Type: Grant
    Filed: April 22, 2013
    Date of Patent: September 29, 2015
    Assignee: Allergan, Inc.
    Inventors: Glenn T. Huang, James A. Burke, Patrick M. Hughes, Kai-Ming Zhang, Ton Lin, Larry A. Wheeler, Rosy Sheng
  • Publication number: 20140364402
    Abstract: The present invention provides, inter alia, a method for identifying an agent that selectively decreases the number of cancer stem cells (CSCs). This method includes (a) contacting a CSC from a population of cells with a candidate agent; and (b) determining whether the candidate agent reduces the survival or growth of the CSC or increases differentiation of the CSC relative to a CSC that has not been contacted with the candidate agent. The method may be used as a high throughput screen.
    Type: Application
    Filed: March 22, 2012
    Publication date: December 11, 2014
    Applicant: THE ROGOSIN INSTITUTE
    Inventors: Barry Smith, Carlos Cordon-Cardo, Daniel Petrylak, Josep Domenech, Mireia Castilla Martin
  • Publication number: 20140357620
    Abstract: There are provided a new dosage regimens for the gamma secretase inhibitor 2,2-Dimethyl-N-((S)-6-oxo-6,7-dihydro-5H-dibenzo[b,d]azepin-7-yl)-N-(2,2,3,3,3-pentafluoro-propyl)-malonamide which maximizes anti-tumor activity while maintaining acceptable toxicity levels.
    Type: Application
    Filed: August 20, 2014
    Publication date: December 4, 2014
    Inventors: John Frederick Boylan, Stanislaw M. Mikulski
  • Publication number: 20140248378
    Abstract: The present invention provides compounds of formula (1) and pharmaceutically acceptable salts thereof, wherein R1, R2, Y and Z are as defined in the specification, processes for their preparation, pharmaceutical compositions containing them and their use in therapy.
    Type: Application
    Filed: July 5, 2012
    Publication date: September 4, 2014
    Applicant: TAKEDA PHARMACEUTICAL COMPANY LIMITED
    Inventors: Xiao-Ling Fan Cockcroft, William Farnaby, Natasha Kinsella, Kevin Merchant, David Miller
  • Publication number: 20140187495
    Abstract: Described are methods for treating cancers, e.g., glioblastoma, including administering an inhibitor of Notch signalling, e.g., a gamma secretase inhibitor, in combination with a chemotherapeutic agent.
    Type: Application
    Filed: December 20, 2013
    Publication date: July 3, 2014
    Applicant: University of Massachusetts
    Inventors: Alonzo H. Ross, Candace Gilbert, Richard Moser
  • Patent number: 8741889
    Abstract: The present invention provides a method for treating a patient having cancer comprising administering to the patient a therapeutically effective amount of compound (1), or a pharmaceutically acceptable salt thereof, having the formula: The present invention also provides a kit containing the above compound.
    Type: Grant
    Filed: April 19, 2012
    Date of Patent: June 3, 2014
    Assignee: Hoffmann-La Roche Inc
    Inventors: John Frederick Boylan, Leopoldo Ladores Luistro, Kathryn Elizabeth Packman
  • Publication number: 20140128357
    Abstract: The disclosure relates to methods of using brassinosteroid compounds, including those defined by formula I or a derivative thereof, for inducing an anabolically favorable state for growth, repair, and maintenance of skeletal muscle and skin.
    Type: Application
    Filed: December 13, 2011
    Publication date: May 8, 2014
    Applicant: Rutgers University
    Inventors: Ilya Raskin, Debora Esposito, Slavko Komarnytsky, Thirumurugan Rathinasabapathy, Leonel Rojo Castillo
  • Patent number: 8691808
    Abstract: The present disclosure provides compounds having affinity for the M2 proton channel, useful for the treatment of viral infections such as influenza, which are of the Formula (I): wherein R1, R2, and Y are as defined herein. Methods of preparing the compounds, pharmaceutical compositions containing the compounds, and methods of using the compounds in the treatment of viral infections such as influenza are also provided.
    Type: Grant
    Filed: May 18, 2012
    Date of Patent: April 8, 2014
    Assignee: Influmedix, Inc.
    Inventors: Jizhou Wang, Xiaodong Fan, Lidia Cristian
  • Publication number: 20130281437
    Abstract: The present invention provides a method for treating a patient having cancer comprising administering to the patient a therapeutically effective amount of compound (1), or a pharmaceutically acceptable salt thereof, having the formula: The present invention also provides a kit containing the above compound.
    Type: Application
    Filed: April 19, 2012
    Publication date: October 24, 2013
    Inventors: John Frederick Boylan, Leopoldo Ladores Luistro, III, Kathyrn Elizabeth Packman
  • Publication number: 20130252930
    Abstract: Provided herein are inhibitors of CYP11B, CYP17, and/or CYP21 enzymes of Formula (Z), (IX), (X), (XI), (XII), (XIII), (XIV), (XV), (XVI), or (XVII). Also described herein are pharmaceutical compositions that include at least one compound described herein and the use of a compound or pharmaceutical composition described herein to treat androgen-dependent diseases, disorders and conditions.
    Type: Application
    Filed: December 16, 2011
    Publication date: September 26, 2013
    Applicant: BIOMARIN PHARMACEUTICAL INC.
    Inventors: Daniel Chu, Bing Wang, Tao Ye
  • Patent number: 8524701
    Abstract: The present invention provides the use in a pharmaceutical composition of a specific cyclic amine derivative, or its pharmaceutically acceptable salts, for the treatment of heart failure of any aetiology.
    Type: Grant
    Filed: June 13, 2008
    Date of Patent: September 3, 2013
    Assignee: Boehringer Ingelheim Pharma GmbH & Co. KG
    Inventors: Brian Guth, Randolph Seidler, Juergen Daemmgen
  • Publication number: 20130217674
    Abstract: Compounds of structure (I): including stereoisomers and pharmaceutically acceptable salts thereof, wherein R1, R2 and A are as defined herein are disclosed. Such compounds have enhanced water solubility and have activity as SHIP1 modulators, and thus may be used to treat any of a variety of diseases, disorders or conditions that would benefit from SHIP1 modulation. Enantioselective methods for preparation of compounds of structure (I), compositions comprising a compound of structure (I) in combination with a pharmaceutically acceptable carrier or diluents and methods of SHIP1 modulation by administration of such compounds to an animal in need thereof are also disclosed.
    Type: Application
    Filed: August 22, 2011
    Publication date: August 22, 2013
    Applicant: THE UNIVERSITY OF BRITISH COLUMBIA
    Inventors: Xiaoxia Wang, Labros George Meimetis, Matthew Bruce Nodwell, Raymond Andersen
  • Publication number: 20130196976
    Abstract: Disclosed are a composition for reducing beta amyloid-induced neurotoxicity by inhibiting ?-secretase activity, comprising a dibenzofuran derivative, and a method for preparing the same. Further disclosed is that the combination of the dibenzofuran derivative with a ?-secretase inhibitor or an anti-inflammatory agent shows higher activity with respect to reducing beta amyloid-induced neurotoxicity.
    Type: Application
    Filed: March 12, 2013
    Publication date: August 1, 2013
    Applicant: PHLORONOL, INC.
    Inventor: PHLORONOL, INC.
  • Publication number: 20130102538
    Abstract: The present invention relates to a method for treating an individual having Alzheimer's Disease by using pharmacological chaperones that bind presenelin and thereby increase ?-secretase activity.
    Type: Application
    Filed: May 4, 2011
    Publication date: April 25, 2013
    Applicant: AMICUS THERAPEUTICS, INC.
    Inventors: Brandon Wustman, Anthony Stevens
  • Patent number: 8377886
    Abstract: Methods are provided for treating and preventing renal disease in a subject by administering a gamma secretase inhibitor or a Notch pathway inhibitor to the subject.
    Type: Grant
    Filed: September 4, 2008
    Date of Patent: February 19, 2013
    Assignee: Albert Einstein College of Medicine of Yeshiva University
    Inventors: Katalin Susztak, Bernhard Bielesz, Thiruvur G. Niranjan
  • Publication number: 20120295886
    Abstract: The present disclosure provides compounds having affinity for the M2 proton channel, useful for the treatment of viral infections such as influenza, which are of the Formula (I): wherein R1, R2, and Y are as defined herein. Methods of preparing the compounds, pharmaceutical compositions containing the compounds, and methods of using the compounds in the treatment of viral infections such as influenza are also provided.
    Type: Application
    Filed: May 18, 2012
    Publication date: November 22, 2012
    Applicant: INFLUMEDIX, INC.
    Inventors: Jizhou Wang, Xiaodong Fan, Lidia Cristian
  • Publication number: 20120238549
    Abstract: The invention provides a compound of Formula (I) pharmaceutically acceptable salts, pro-drugs, biologically active metabolites, stereoisomers and isomers thereof wherein the variable are defined herein. The compounds of the invention are useful for treating immunological and oncological conditions.
    Type: Application
    Filed: March 15, 2012
    Publication date: September 20, 2012
    Applicant: ABBOTT LABORATORIES
    Inventors: Kevin P. Cusack, Thomas D. Gordon, David C. Ihle, Martin E. Hayes, Eric C. Breinlinger, Anna M. Ericsson, Bin Li, Lei Wang, Gloria Y. Martinez, Andrew Burchat, Adrian D. Hobson, Kelly D. Mullen, Michael Friedman, Michael J. Morytko
  • Publication number: 20120230951
    Abstract: The present invention provides compounds, compositions and methods for the treatment of hepatitis C virus (HCV) infection. Also disclosed are pharmaceutical compositions containing such compounds and methods for using these compounds in the treatment of HCV infection.
    Type: Application
    Filed: March 8, 2012
    Publication date: September 13, 2012
    Inventors: Muzaffar Alam, Steven Joseph Berthel, John A. Brinkman, Ronald Charles Hawley, Hongju Li, Wylie Solang Palmer, Sherrie Pietranico-Cole, Ramakanth Sarabu, Mark Smith, Sung-Sau So, Lin Yi, Yansheng Zhai, Qiang Zhang, Shu-Hai Zhao
  • Publication number: 20120225860
    Abstract: There are provided a new dosage regimens for the gamma secretase inhibitor 2,2-Dimethyl-N-((S)-6-oxo-6,7-dihydro-5H-dibenzo[b,d]azepin-7-yl)-N?-(2,2,3,3,3-pentafluoro-propyl)-malonamide which maximizes anti-tumor activity while maintaining acceptable toxicity levels.
    Type: Application
    Filed: February 20, 2012
    Publication date: September 6, 2012
    Inventors: John Frederick Boylan, Stanislaw Mikulski
  • Publication number: 20120184529
    Abstract: The present invention relates to a combination therapy of 2-Chloro-N-(4-chloro-pyridin-2-yl-phenyl)-4-methanesulfonyl-benzamide and 2,2-Dimethyl-N-((S)-6-oxo-6,7-dihydro-5H-dibenzo[b,d]azepin-7-yl)-N?-(2,2,3,3,3-pentafluoro-propyl)-malonamide for treating a patient suffering from a proliferative disorder.
    Type: Application
    Filed: January 3, 2012
    Publication date: July 19, 2012
    Inventors: Mark D. DeMario, Stanislaw M. Mikulski
  • Patent number: 8217030
    Abstract: Association of a sinus node If current inhibitor and a ?-blocker and also pharmaceutical compositions containing it. Medicinal products containing the same which are useful in treating angina pectoris, ischaemia, and heart failure.
    Type: Grant
    Filed: February 11, 2009
    Date of Patent: July 10, 2012
    Assignee: Les Laboratoires Servier
    Inventors: Guy Lerebours-Pegeonniere, Jean-Henri Calvet
  • Publication number: 20110287025
    Abstract: The present invention relates to a method for determining a subject's resistance to treatment with 2,2-dimethyl-N—((S)-6-oxo-6,7-dihydro-5H-dibenzo[b,d]azepin-7-yl)-N?-(2,2,3,3,3-pentafluoro-propyl)-malonamide by measuring the levels a biomarker or biomarkers present in a biological sample obtained from the subject, the biomarker being IL6 and/or IL8. The present invention also relates to a combination therapy for a patient suffering from a proliferative disorder comprising administering to the patient 2,2-Dimethyl-N—((S)-6-oxo-6,7-dihydro-5H-dibenzo[b,d]azepin-7-yl)-N?-(2,2,3,3,3-pentafluoro-propyl)-malonamide and an anti-IL6 and/or an anti-IL8 agent.
    Type: Application
    Filed: May 2, 2011
    Publication date: November 24, 2011
    Inventors: John Frederick Boylan, Wei He
  • Publication number: 20110245233
    Abstract: This invention provides, but is not limited to, novel oleanolic acid derivatives having the formula: wherein the variables are defined herein. Also provided are pharmaceutical compositions, kits and articles of manufacture comprising such compounds, methods and intermediates useful for making the compounds, and methods of using the compounds and compositions.
    Type: Application
    Filed: February 23, 2011
    Publication date: October 6, 2011
    Inventors: Eric Anderson, Xin Jiang, Xiaofeng Liu, Melean Visnick
  • Patent number: 8022203
    Abstract: New aminoalkoxyimino derivatives at position 3 of substituted B-homoandrostanes and B-heteroandrostanes, processes for their preparation, and to pharmaceutical compositions containing them for the treatment of cardiovascular disorders, such as heart failure and hypertension. In particular compounds having the general formula (I) are described, where the radicals have the meanings described in detail in the application.
    Type: Grant
    Filed: May 31, 2007
    Date of Patent: September 20, 2011
    Assignee: Sigma-Tau Industrie Farmaceutiche Riunite S.p.A.
    Inventors: Alberto Cerri, Barbara Moro, Maco Torri, Giulio Carzana, Giuseppe Bianchi, Mara Ferrandi, Patrizia Ferrari, Maria Pia Zappavigna, Leonardo Banfi, Giuseppe Giacalone
  • Publication number: 20110178065
    Abstract: Provided herein are inhibitors of CYP17 enzyme. Also described herein are pharmaceutical compositions that include at least one compound described herein and the use of a compound or pharmaceutical composition described herein to treat androgen-dependent diseases, disorders and conditions.
    Type: Application
    Filed: January 13, 2011
    Publication date: July 21, 2011
    Applicant: BIOMARIN PHARMACEUTICAL INC.
    Inventors: Daniel Chu, Bing Wang, Tao Ye
  • Publication number: 20110150835
    Abstract: The present invention discloses novel compounds which have HCV protease inhibitory activity as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising such compounds as well as methods of using them to treat disorders associated with the HCV protease.
    Type: Application
    Filed: October 31, 2007
    Publication date: June 23, 2011
    Inventors: Srikanth Venkatraman, F. George Njoroge, Wanli Wu, Viyyoor M. Girijavallabhan, Brian A. McKittrick, Jing Su, Francisco Velazquez, Patrick A. Pinto
  • Patent number: 7915280
    Abstract: This invention relates to compounds, pharmaceutical compositions, and methods of using the disclosed compounds for inhibiting PARP.
    Type: Grant
    Filed: August 30, 2005
    Date of Patent: March 29, 2011
    Assignee: Eisai Inc.
    Inventors: Dana Victor Ferraris, Jia-He Li, Vincent Kalish, Jie Zhang
  • Publication number: 20110033463
    Abstract: A device is configured to remove a target molecule from a bodily fluid of a subject and to deliver a therapeutic agent to the subject. Such a device may be used for treatment of a disease associated with amyloid beta accumulation in the subject. Agents selected from the group consisting of an ApoE-modulating agent; a RAGE inhibitor; a ?-secretase 1 (BACE1) inhibitor; a ?-secretase inhibitor; a muscarinic receptor subtype 1 (M1) agonists; a growth factor; an enzyme capable of degrading amyloid beta; a mitochondrial antioxidant; insulin; and an inhibitor of tumor necrosis factor (TNF) may be administered directly to the central nervous system of a subject for treatment of a disease associated with amyloid beta accumulation.
    Type: Application
    Filed: August 6, 2010
    Publication date: February 10, 2011
    Applicant: MEDTRONIC, INC.
    Inventors: Deepak R. Thakker, Lisa L. Shafer
  • Publication number: 20100292157
    Abstract: The invention relates generally to novel compositions and methods comprising a cyclohexanehexol and a secretase inhibitor. The compositions and methods provide beneficial effects, in particular sustained beneficial effects, in the treatment of diseases involving a disorder in protein folding and/or aggregation, and/or amyloid formation, deposition, accumulation, or persistence, such as Alzheimer's disease and related neurodegenerative disorders.
    Type: Application
    Filed: November 22, 2007
    Publication date: November 18, 2010
    Inventor: Antonio Cruz
  • Publication number: 20100226944
    Abstract: The present invention relates to a process for the preparation of controlled-release solid oral pharmaceutical formulations of oxcarbazepine, and the pharmaceutical formulations obtainable by said process.
    Type: Application
    Filed: July 23, 2008
    Publication date: September 9, 2010
    Applicant: ARCHIMICA S.R.L.
    Inventors: Giovanni Sanso', Aldo Banfi, Giorgio Bertolini, Claudio Silva
  • Publication number: 20100222283
    Abstract: Methods are provided for treating and preventing renal disease in a subject by administering a gamma secretase inhibitor or a Notch pathway inhibitor to the subject.
    Type: Application
    Filed: September 4, 2008
    Publication date: September 2, 2010
    Inventors: Katalin Susztak, Bernhard Bielesz, Thiruvur G. Niranjan
  • Publication number: 20100216772
    Abstract: The present invention relates to compounds of the general formula (IV) and (II) and salts and physiologically functional derivatives thereof, wherein X is C—R8 or N; and Z is independently one of the following groups:
    Type: Application
    Filed: October 5, 2004
    Publication date: August 26, 2010
    Inventors: Stefano Pegoraro, Martin Lang, Juliane Feurle, Jürgen Krauss
  • Patent number: 7767664
    Abstract: The present invention relates to a new class of plant growth regulators. In particular, the invention relates to fused azepinone derivative of general formula (I) or an agriculturally acceptable salt thereof wherein X is CO2R2 or H; Y is OH; NHNR3R4, NHNHC(?Z)NR5R6 or NHNHC(?Z)CR7R8R9; or X and Y together with the two carbon atoms to which they are attached form a ring of formula (A) and a method for treatment of plants with such compounds in order to induce growth regulating responses.
    Type: Grant
    Filed: April 30, 2005
    Date of Patent: August 3, 2010
    Assignee: Bayer CropScience AG
    Inventors: Henricus M. M. Bastiaans, Günter Donn, Nathalie Knittel, Arianna Martelletti, Richard Rees, Michael Schwall, Ryan Whitford
  • Publication number: 20100190688
    Abstract: Compounds, compositions and methods for treatment of hyperproliferative diseases, such as cancer are provided.
    Type: Application
    Filed: July 12, 2005
    Publication date: July 29, 2010
    Inventors: Bin Chao, Thomas L. Deckwerth, Paul S. Furth, Steven D. Linton, Alfred P. Spada, Brett R. Ullman, Michael I. Weinhouse
  • Publication number: 20100190752
    Abstract: A composition of matter comprising in combination as component (a) at least one 3-(3-dimethylamino-1-ethyl-2-methyl-propyl)-phenol compound, and as component (b) at least one antiepileptic, a pharmaceutical formulation and a dosage form comprising said composition of matter, and a method of treating pain, e.g. neuropathic pain, in which components (a) and (b) are administered simultaneously or sequentially to a mammal, whereby component (a) may be administered before or after component (b) and whereby components (a) or (b) are administered to the mammal either via the same or a different pathway of administration.
    Type: Application
    Filed: January 26, 2010
    Publication date: July 29, 2010
    Applicant: Gruenenthal GmbH
    Inventors: Klaus Schiene, Petra Bloms-Funke, Thomas Christoph
  • Publication number: 20100069359
    Abstract: Compounds of formula I: (wherein variables A1, A2, A3, G1, G2, G3, J, m, n, p, R1, R2, R3, R4 and Y are as described herein) which are antagonists of CGRP receptors and which are useful in the treatment or prevention of diseases in which the CGRP is involved, such as migraine. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which CGRP is involved.
    Type: Application
    Filed: December 5, 2007
    Publication date: March 18, 2010
    Inventors: Ian M. Bell, Harold G. Selnick
  • Publication number: 20100041639
    Abstract: This invention relates to novel cyclic malonamides having the formula (I): to their pharmaceutical compositions and to their methods of use. These novel compounds inhibit the processing of amyloid precursor protein and, more specifically, inhibit the production of A?-peptide, thereby acting to prevent the formation of neurological deposits of amyloid protein. More particularly, the present invention relates to the treatment of neurological disorders related to ?-amyloid production such as Alzheimer's disease and Down's Syndrome.
    Type: Application
    Filed: October 21, 2009
    Publication date: February 18, 2010
    Applicant: BRISTOL-MYERS SQIBB PHARMA COMAPNY
    Inventors: Richard E. Olson, Michael G. Yang
  • Publication number: 20100009966
    Abstract: This invention relates to novel lactams of Formula (I): having drug and bio-affecting properties, their pharmaceutical compositions and methods of use. These novel compounds inhibit the processing of amyloid precursor protein and, more specifically, inhibit the production of A?-peptide, thereby acting to prevent the formation of neurological deposits of amyloid protein. More particularly, the present invention relates to the treatment of neurological disorders related to ?-amyloid production such as Alzheimer's disease and Down's Syndrome.
    Type: Application
    Filed: September 15, 2009
    Publication date: January 14, 2010
    Applicant: BRISTOL-MYERS SQUIBB PHARMA COMPANY
    Inventors: Qi HAN, Hong Liu, Richard E. Olson, Michael G. Yang
  • Publication number: 20090281081
    Abstract: Disclosed are novel compounds and a method of treating a disease associated with aberrant leukocyte recruitment and/or activation. The method comprises administering to a subject in need an effective amount of a compound represented by: or physiologically acceptable salt thereof.
    Type: Application
    Filed: May 6, 2009
    Publication date: November 12, 2009
    Inventors: Jay R. Luly, Yoshisuke Nakasato, Etsuo Ohshima, Geraldine C. B. Harriman, Kenneth G. Carson, Shomir Ghosh, Amy M. Elder, Karen M. Mattia
  • Publication number: 20090192140
    Abstract: Disclosed herein is an isomer, enantiomer, diastereoisomer or tautomer of a compound represented by Formula I: or a prodrug, or a pharmaceutically acceptable salt, or labeled with a detectable label or an affinity tag thereof; wherein R1, R1a, R100, R100a, R2, R200, W, B, and W1 are defined herein. Also disclosed are methods of using compounds of Formula I to treat proliferative disorders such as cancer.
    Type: Application
    Filed: May 16, 2007
    Publication date: July 30, 2009
    Applicant: Aegera Therapeutics Inc.
    Inventors: Alain Laurent, Scott Jarvis, Patrick Bureau, Alain Boudreault, James Jaquith
  • Patent number: 7550453
    Abstract: The invention relates particularly to 2-alkoxy-3,4,5-trihydroxy-alkylamides, preparation thereof, compositions containing them and use thereof as a medicament, particularly as anti-cancer agents.
    Type: Grant
    Filed: May 24, 2007
    Date of Patent: June 23, 2009
    Assignee: Aventis Pharma SA
    Inventors: Jidong Zhang, Neerja Bhatnagar, Jean-Marie Ruxer
  • Patent number: 7544679
    Abstract: The invention relates to 6-oxo-6,7-dihydro-5H-dibenzo[b,d]azepin-7-yl derivatives of formula I wherein R1, R2 and R3 are as defined herein. The compounds are ?-secretase inhibitors useful in the treatment of Alzheimer's disease or common cancer, including, but not limited to, cervical carcinomas and breast carcinomas and malignancies of the hematopoietic system.
    Type: Grant
    Filed: January 25, 2008
    Date of Patent: June 9, 2009
    Assignee: Hoffman-La Roche Inc.
    Inventors: Alexander Flohr, Roland Jakob-Roetne, Wolfgang Wostl
  • Publication number: 20090111793
    Abstract: This invention relates to novel lactams having the formula (I): to their pharmaceutical compositions and to their methods of use. These novel compounds inhibit the processing of amyloid precursor protein and, more specifically, inhibit the production of A?-peptide, thereby acting to prevent the formation of neurological deposits of amyloid protein. More particularly, the present invention relates to the treatment of neurological disorders related to ?-amyloid production such as Alzheimer's disease and Down's Syndrome.
    Type: Application
    Filed: September 9, 2008
    Publication date: April 30, 2009
    Applicant: BRISTOL-MYERS SQUIBB PHARMA COMPANY
    Inventors: Richard E. Olson, Hong Liu, Lorin A. Thompson
  • Publication number: 20090069293
    Abstract: This invention relates to novel lactams having the formula (I): to their pharmaceutical compositions and to their methods of use. These novel compounds inhibit the processing of amyloid precursor protein and, more specifically, inhibit the production of A?-peptide, thereby acting to prevent the formation of neurological deposits of amyloid protein. More particularly, the present invention relates to the treatment of neurological disorders related to ?-amyloid production such as Alzheimer's disease and Down's Syndrome.
    Type: Application
    Filed: October 20, 2008
    Publication date: March 12, 2009
    Applicant: Bristol-Myers Squibb Pharma Company
    Inventor: Richard E. Olson
  • Patent number: 7501405
    Abstract: Combination therapy comprising the administration of an 11?-hydroxysteroid dehydrogenase type 1 inhibitor and an antihypertensive agent useful for treating, preventing and reducing the risk of developing insulin resistance, dyslipidemia, obesity, hypertension and other related diseases and disorders.
    Type: Grant
    Filed: October 11, 2005
    Date of Patent: March 10, 2009
    Assignee: High Point Pharmaceuticals, LLC
    Inventors: Gita Camilla Tejlgaard Kampen, Henrik Sune Andersen
  • Publication number: 20090062256
    Abstract: This invention relates to novel lactams having the Formula (I): to their pharmaceutical compositions and to their methods of use. These novel compounds inhibit the processing of amyloid precursor protein and, more specifically, inhibit the production of A?-peptide, thereby acting to prevent the formation of neurological deposits of amyloid protein. More particularly, the present invention relates to the treatment of neurological disorders related to ?-amyloid production such as Alzheimer's disease and Down's Syndrome.
    Type: Application
    Filed: October 24, 2008
    Publication date: March 5, 2009
    Applicant: BRISTOL-MYERS SQUIBB PHARMA COMPANY
    Inventor: Richard E. Olson
  • Publication number: 20080312210
    Abstract: The present invention provides the use in a pharmaceutical composition of a specific cyclic amine derivative, or its pharmaceutically acceptable salts, for the treatment of heart failure of any aetiology.
    Type: Application
    Filed: June 13, 2008
    Publication date: December 18, 2008
    Applicant: Boehringer Ingelheim Pharma GmbH & Co. KG
    Inventors: Brian GUTH, Randolph SEIDLER, Juergen DAEMMGEN