Abstract: A bicyclic heteroaromatic compound according to general formula I, or a pharmaceutically acceptable salt thereof, wherein R1 is (3–8C)cycloalkyl, (2–7C)heterocycloalkyl, (6–14C)aryl or (4–13C)heteroaryl; all optionally substituted with one or more substituents; R2 is (1–4C)alkyl, (2–4C)alkenyl, (2–4C)alkynyl, (6–14C)aryl or (4–13C)heteroaryl; R3 is (1–8C)alkyl, (3–8C)cycloalkyl, (2–7C)heterocycloalkyl, (6–14C)aryl or (4–13C)heteroaryl; Y is CH or N; Z is NH2 or OH; A is S, N(H), N(R), O or a bond and B is N(H), O or a bond; X1—X2 is C?C, C(O)—NH, NH—C(O), C(O)—O, O—C(O), C?N, N?C or S or O. The compounds of the invention can be used in fertility regulation therapies.
Type:
Grant
Filed:
September 17, 2001
Date of Patent:
June 12, 2007
Assignee:
N.V. Organon
Inventors:
Cornelis Marius Timmers, Willem Frederik Johan Karstens
Abstract: A process is disclosed for releasing proteins from cells and/or inactivating viruses. In the process, a host cell containing a protein of interest is contacted with a solution of an effective amount of a detergent.
Abstract: The invention relates to an isolated polynucleotide sequence comprising a nucleic acid sequence encoding the amino acid sequence of KshA protein or of KshB protein, encoded by nucleotides 499–1695 of SEQ ID NO: 1 or by nucleotides 387–1427 of SEQ ID NO:2, respectively, and functional homologues thereof. The polynucleotides of the invention can be used to construct genetically modified microorganisms blocked in 3-ketosteroid 9?-hydroxylase activity, which are useful in the microbial degradation of steroids to accumulate certain steroid products.
Type:
Grant
Filed:
February 19, 2003
Date of Patent:
May 29, 2007
Assignee:
N.V. Organon
Inventors:
Robert Van Der Geize, Peter Van Der Meijden, Gerda Hessels, Lubbert Dijkhuizen
Abstract: The present invention provides isolated polynucleotides encoding a receptor gene called GPR50 having at least one polymorphic sites. It furthermore provides a method for analyzing polymorphic sites in the receptor gene. Certain of these polynucleotides having a polymorphic site (allelic variants) are found to be more prevelant in a population of patients with clinical Bipolar Depression compared to a control population. A method for the genetic testing of Bipolar Depression is a further embodiment of the present invention. Furthermore, polynucleotides encompassing these polymorphic sites, the invariant distal or proximal to the polymorphic site localized polynucleotides as well as the polynucleotides encoding CPR50 are part of the invention. The present invention also provides a recombinant cell line expressing these novel receptors at appropriate levels such that novel compounds active at these receptors may be identified for therapeutic use.
Abstract: The present invention relates to a 9-azabicyclo[3.3.1]nonane derivative of formula I, wherein each of the substituents is given the definition as set forth in the specification and claims, or a pharmaceutically acceptable salt or solvate thereof. The invention also relates to pharmaceutical compositions comprising said 9-azabicyclo[3.3.1]nonane derivatives and to their use in therapy.
Type:
Application
Filed:
September 29, 2006
Publication date:
May 17, 2007
Applicant:
N.V. Organon
Inventors:
Susan Napier, Matilda Bingham, Margaret Huggett, Mark Huggett, Yasuko Kiyoi, Olaf Nimz
Abstract: Disclosed herein are 4-phenyl-6-substituted-pyrimidine-2-carbonitrile derivatives having Formula I, wherein each of the substituents is given the definition as set forth in the specification and claims; or a pharmaceutically acceptable salt thereof. Also disclosed are pharmaceutical compositions comprising these 4-phenyl-6-substituted-pyrimidine-2-carbonitrile derivatives and use of these 4-phenyl-6-substituted-pyrimidine-2-carbonitrile derivatives for the treatment of cathepsin K and cathepsin S related disorders, e.g. osteoporosis, atherosclerosis, inflammation and immune disorders such as rheumatoid arthritis and chronic pain.
Abstract: There is provided a polymer having a side chain of general formula (I) in which R may be any suitable alkyl, oxyalkyl, aryl or oxyaryl linking group R is preferably C1-6 alkyl (especially —CH2—), a benzene group or a group —CH2—O-Phe-. Generally, the side chain will be attached to an ethylene moiety forming part of the backbone of the polymer. Preferred polymers include polystyrene. The polymer is useful as a support for solid phase chemical reactions especially combinatorial chemical synthesis.
Type:
Grant
Filed:
March 12, 2004
Date of Patent:
February 27, 2007
Assignee:
N.V. Organon
Inventors:
David Gani, Friedrich E. Kroll, Michael J. Plater, John R. Morphy, David C. Rees