Abstract: The present invention relates to 1-arylsulfonyl-3 substituted indole or indoline derivatives having the general formula (I) (I) wherein the dotted line represents an optional bond; n is 0 or 1; m is 0-5 and Ar, R6-R11 are defined in the description. The invention further relates to pharmaceutical compositions comprising said derivatives, and to the use of these 1-arylsulfonyl-3-substituted indole or indoline derivatives in the treatment of central nervous disorders such as psychosis, schizophrenia, manic depressions, depressions, neurological disorders, cognitive enhancement, Parkinson's disease, amyotrophic lateral sclerosis, Alzheimer's disease and Huntington's disease.
Type:
Grant
Filed:
February 5, 2003
Date of Patent:
November 23, 2010
Assignee:
N.V. Organon
Inventors:
Daniel Spinks, Richard E. Armer, David J. Miller, Zoran Rankovic, Gayle Spinks, Jordi Mestres, David Robert Jaap
Abstract: Disclosed herein are quinazolinone or isoquinolinone derivatives of formula I, or pharmaceutically acceptable salts or solvates thereof, wherein each of the substituents is given the definition as set forth in the specification and claims. Also disclosed are pharmaceutical compositions comprising quinazolinone or isoquinolinone according to the present invention and its use in therapy.
Type:
Grant
Filed:
September 10, 2007
Date of Patent:
October 26, 2010
Assignee:
N.V. Organon
Inventors:
Jeffrey Letourneau, Patrick Jokiel, Susan Elizabeth Napier, Koc-Kan Ho, Michael Ohlmeyer, Duncan Robert McArthur, Fiona Jeremiah, Paul David Ratcliffe, Jurgen Schulz
Abstract: The present invention relates to a heterocyclic derivative according to formula I wherein the variables are defined as in the specification, or to a pharmaceutically acceptable salt or solvate thereof. The present invention also relates to a pharmaceutical composition comprising said heterocyclic derivatives and to their use in therapy, for instance in the treatment or prevention of psychiatric diseases where an enhancement of synaptic responses mediated by AMPA receptors is required, including schizophrenia, depression and Alzheimer's disease.
Type:
Grant
Filed:
June 29, 2007
Date of Patent:
October 26, 2010
Assignee:
N.V. Organon
Inventors:
Kevin James Gillen, Craig Jamieson, John Kinnaird Ferguson MacLean, Elizabeth Margaret Moir, Zoran Rankovic
Abstract: The invention provides a method of treatment of hot flush with S-mirtazapine and the use of S-mirtazapine for the manufacture of a medicament for the treatment of hot flush.
Type:
Application
Filed:
July 1, 2010
Publication date:
October 21, 2010
Applicant:
N.V. Organon
Inventors:
Bernardus Wijnand Mathys Marie Peeters, Anton Egbert Peter Adang
Abstract: The compounds of the subject invention have a structure according to formula I: wherein each of the substituents is given the definition as set forth in the specification and claims, or a salt or hydrate form thereof.
Type:
Grant
Filed:
April 21, 2005
Date of Patent:
October 12, 2010
Assignee:
N.V. Organon
Inventors:
Jaap Van Der Louw, Neeltje Miranda Teerhuis, Johannes Petrus Maria Lommerse, Herman Thijs Stock, Pedro Harold Han Hermkens
Abstract: The present invention relates to 2-(4-oxo4H-quinazolin-3-yl) acetamicle derivatives of formula (I), and to their use as vasopressin V3 antagonists, particularly for the treatment of depression.
Type:
Grant
Filed:
March 10, 2006
Date of Patent:
October 5, 2010
Assignee:
N.V. Organon
Inventors:
Jeffrey Letourneau, Christopher Riviello, Koc-Kan Hoc, Jui-Hsiang Chan, Michael Ohlmeyer, Patrick Jokiel, Irina Neagu, John Richard Morphy, Susan Elizabeth Napier
Abstract: The invention discloses a steroid compound having the formula (1): wherein dotted bonds represent optional double bonds; R6 is H, ?CH2, or —CH3, or —CH2—CH3; R7 is H, C1-4-alkyl, C2-5 alkenyl or C2-5-alkynyl, wherein the alkyl, alkenyl or alkynyl group may be substituted with 1 to 3 halogen atoms independently chosen from the group of fluorine or chlorine atoms; R11 is H, C1-4-alkyl, C2-4-alkenyl, C2-4-alkynyl or C1-4-alkylidene, wherein the alkyl, alkenyl, alkynyl or alkylidene group may be substituted with 1 to 3 halogen atoms independently chosen from the group of fluorine or chlorine atoms; E represents together with carbon atoms 16 and 17 of the steroid skeleton a four to seven-membered ring, said ring being ? and in cis-configuration with respect to the steroid skeleton, optionally comprising one or two endocyclic bonds; or a prodrug thereof. Such compounds can be used in therapy and for methods for selective modification of the activity of estrogen receptors.
Abstract: The invention relates to a novel process for the preparation of asenapine, i.e. trans-5-chloro-2-methyl-2,3,3a,12b-tetrahydro-1H-dibenz[2,3:6,7]oxepino[4,5-c]pyrrole, as well as to novel intermediate products for use in said process.
Type:
Application
Filed:
May 24, 2010
Publication date:
September 16, 2010
Applicant:
N.V. Organon
Inventors:
Gerardus Johannes Kemperman, Timothy Lee Stuk, Jacobus Johannes Maria Van Der Linden
Abstract: This invention provides non-steroidal compounds with affinity for the androgen receptor and utility for androgen-receptor related treatments, having a structure according to the formula or a salt or hydrate form thereof.
Type:
Grant
Filed:
November 3, 2003
Date of Patent:
September 14, 2010
Assignee:
N.V. Organon
Inventors:
Pedro Harold Han Hermkens, Herman Thijs Stock, Jaap Van Der Louw, Neeltje Miranda Teerhuis, Johannes Petrus Maria Lommerse
Abstract: The invention relates to tricyclic 1-[(indol-3-yl)carbonyl]piperazine derivative having the general Formula (I) wherein X is CH2, O or S; R represents 1-3 substituents independently selected from H, (C1-4)alkyl, (C1-4)alkyloxy and halogen; R1 is (C5-8)cycloalkyl; R2 is H or (C1-4)alkyl; R3, R3?, R4? R4?, R5, R5? and R6? are independently hydrogen or (C1-4)-alkyl, optionally substituted with (C1-4)alkyloxy, OH or halogen; R6 is hydrogen or (C1-4)alkyl, optionally substituted with (C1-4)alkyloxy, OH or halogen; or R6 forms together with R7 a 4-7 membered saturated heterocyclic ring, optionally containing a further heteroatom selected from O and S; R7 forms together with R6 a 4-7 membered saturated heterocyclic ring, optionally containing a further heteroatom selected from O and S; or R7 is H, (C1-4)alkyl or (C3-5)cycloalkyl, the alkyl groups being optionally substituted with OH, halogen or (C1-4)alkyloxy; or a pharmaceutically acceptable salt thereof.
Abstract: Compositions and methods are provided for enhancing the survival and promoting the maturation of mammalian oocytes, zygotes and preimplantation embryos. BDNF or BDNF agonists may be administered to an individual, or to cells in vitro, to enhance cellular maturation, embryo growth and fertilization. Accordingly, compositions comprising BDNF are herein presented for use in promoting in vivo oocyte maturation as well as for use as a component in culture media for promoting preimplantation maturation of zygotes and embryos, for instance, for use with in vitro fertilization procedures and for the production of stem cells. Additionally, compounds that interfere with the binding of BDNF to its receptor may be administered to an individual to prevent oocyte maturation, thereby acting as a contraceptive. The BNDF receptor, TrkB, and BDNF also find use in the screening and design of agonists and antagonists for use in the methods of the invention.
Type:
Grant
Filed:
June 13, 2007
Date of Patent:
July 27, 2010
Assignees:
The Board of Trustees of the Leland Stanford Junior University, N.V. Organon
Inventors:
Kazuhiro Kawamura, Aaron J. W. Hsueh, Sabine M. Mulders
Abstract: Disclosed herein are indole derivatives of the formula (I) wherein each of the substitutents is given the definition as set forth in the specification and claims. Also disclosed are pharmaceutical compositions containing the indole derivatives and use of the derivatives for the treatment of pain.
Type:
Grant
Filed:
August 18, 2006
Date of Patent:
July 27, 2010
Assignee:
N.V. Organon
Inventors:
Paul David Ratcliffe, Julia Adam-Worrall, Angus John Morrison, Stuart John Francis, Takao Kiyoi
Abstract: The invention relates to a novel process for the preparation of asenapine, i.e. trans-5-chloro-2-methyl-2,3,3a,12b-tetrahydro-1H-dibenz[2,3:6,7]oxepino[4,5-c]pyrrole, as well as to novel intermediate products for use in said process.
Type:
Grant
Filed:
July 3, 2007
Date of Patent:
July 6, 2010
Assignee:
N.V. Organon
Inventors:
Gerardus Johannes Kemperman, Timothy Lee Stuk, Jacobus Johannes Maria Van Der Linden
Abstract: The invention relates to an orthorhombic crystal form of compound trans-5-chloro-2,3,3a,12b-tetrahydro-2-methyl-1H-dibenz [2,3:6,7]oxepino[4,5-c]pyrrole (Z)-2-butenedioate, to methods for the preparation of this crystal form and to pharmaceutical compositions comprising an orthorhombic crystal form.
Abstract: The present invention provides compounds according to general Formula (I), a prodrug thereof, a pharmaceutically acceptable salt thereof, or a pharmaceutically acceptable salt of a prodrug thereof. More particularly, the present invention provides high affinity non-steroidal compounds which are agonists, partial agonists or antagonists of the progesterone receptor.
Type:
Grant
Filed:
April 1, 2003
Date of Patent:
June 15, 2010
Assignee:
N.V. Organon
Inventors:
Pedro Harold Han Hermkens, Hans Lucas, Paul Peter Marie Antonius Dols, Johannes Bernardus Maria Rewinkel, Brigitte Johanna Bernita Folmer
Abstract: The present invention relates to plexin D1 for use as a targetable protein in the treatment or diagnosis of disorders that involve expression of plexin D1. Diagnosis is suitably effected by detecting the presence of plexin D1 in the body or a bodily tissue or fluid, whereas treatment is effected by targeting plexin D1 for delivery of therapeutics to the site where treatment is needed. The invention further relates to the use of molecules that bind plexin D1, a nucleic acid encoding plexine D1 or a ligand of plexin D1 for the preparation of a therapeutical composition for the treatment or diagnosis of disorders that involve expression of plexin D1. The disorders comprise disorders in which plexin D1 is expressed on tumor cells, tumor blood vessels or activated macrophages.
Type:
Application
Filed:
July 20, 2006
Publication date:
May 13, 2010
Applicant:
N.V. Organon
Inventors:
Wilhelmus Petrus Johannes Leenders, Ilse Roodink, Jozef Maria Hendrik Raats
Abstract: This invention relates to an extended release formulation comprising a solid non-steroidal non-ionized hydrophilic drug, having a molecular weight below 500 Dalton and having a solubility of at least 0.1 wt % in ethylene vinyl acetate copolymer having a vinyl acetate content of 28%, which formulation is a vaginal device having a skin and which device comprises an inner compartment made of a thermoplastic polymer, which polymer is containing the drug. The polymer is preferably made of ethylene-vinyl acetate copolymer.
Abstract: This invention relates to novel 1,5,7-trisubstituted benzimidazole derivatives, pharmaceutical compositions containing these compounds, and methods of treatment therewith. The compounds of the invention are useful in the treatment of central nervous system diseases and disorders, which are responsive to modulation of the GABAA receptor complex.
Type:
Grant
Filed:
October 20, 2004
Date of Patent:
April 20, 2010
Assignees:
N. V. Organon, Neurosearch A/S
Inventors:
Niall Morton Hamilton, Susan Elizabeth Napier, Morag Ann MacCall Easson, Andrew John Cooke, Lene Teuber, Naheed Mirza, Frank Wätjen
Abstract: Disclosed herein are indole derivatives of the formula (I) wherein each of the substitutents is given the definition as set forth in the specification and claims. Also disclosed are pharmaceutical compositions containing the indole derivatives and use of the derivatives for the treatment of pain.
Type:
Grant
Filed:
February 28, 2005
Date of Patent:
April 20, 2010
Assignee:
N.V. Organon
Inventors:
Julia Adam-Worrall, Angus John Morrison, Grant Wishart, Takao Kiyoi, Duncan Robert McArthur
Abstract: The invention makes a 16?-substituted steroidal compound available having formula 1, wherein the dotted ring is a fully saturated, a fully aromatic or a saturated ring with a ?5-10 double bond; R1 is (C1-C3)alkyl or (C2-C3)alkenyl, and each of these groups can be substituted with one or more halogens; R2 is (C1-C4;)alkyl, (C2-C4)alkenyl or methylene, and each of these groups can be substituted with one or more halogens; R3 is methyl or ethyl; or a prodrug thereof, which compound can be used for an estrogen receptor ? selective treatment
Type:
Grant
Filed:
July 23, 2001
Date of Patent:
April 13, 2010
Assignee:
N.V. Organon
Inventors:
Jordi Mestres, Hubert Jan Jozef Loozen, Gerrit Herman Veeneman