Patents Represented by Attorney, Agent or Law Firm Susan Hess
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Patent number: 7507824Abstract: The present invention relates to spiro[2H-1-benzopyran-2,4?-piperidine] derivatives having general formula (I), or a pharmaceutically acceptable salt thereof. The invention also relates to pharmaceutical compositions comprising said derivatives, as well as to the use of these spiro[2H-1-benzopyran-2,4?-piperidine] derivatives in therapy, more specifically for the treatment of CNS disorders.Type: GrantFiled: August 8, 2003Date of Patent: March 24, 2009Assignee: N.V. OrganonInventors: Samuel George Gibson, David John Miller
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Patent number: 7504390Abstract: The present invention relates to benzoxazepine derivative having the general formula I, wherein X represents CO or SO2; R1, R2, R3 and R4 are independently selected from H, (C1-4)alkyl, (C1-4)alkyloxy, (C1-4)alkyloxy(C1-4)alkyl, halogen, nitro, cyano, NR8R9, NR8COR10, and CONR8R9, R5, R6 and R7 are independently H or (C1-4)alkyl; R8 and R9 are independently H or (C1-4)alkyl; or R8 and R9 form together with the nitrogen atom to which they are bound a 5- or 6-membered saturated heterocyclic ring, optionally containing a further heteroatom selected from O, S or NR11; R10 is (C1-4)alkyl; R11 is (C1-4)alkyl; A represents the residue of a 4-7 membered saturated heterocyclic ring, optionally containing an oxygen atom, the ring being optionally substituted with 1-3 substituents selected from (C1-4)alkyl, (C1-4)alkyloxy, hydroxy, halogen and oxo; or a pharmaceutically acceptable salt thereof.Type: GrantFiled: October 25, 2007Date of Patent: March 17, 2009Assignee: N.V. OrganonInventors: Simon James Anthony Grove, Mingqiang Zhang, Mohammad Shahid
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Patent number: 7482469Abstract: The invention relates to 2-(benzimidazol-1-yl)-acetamide bisaryl derivative having the general Formula I wherein n is 0 or 1; Ar1 represents a diradical derived from a 5- or-6-membered aromatic ring, optionally comprising 1-3 heteroatoms selected from N, O and S, said ring being optionally substituted with (C1-4)alkyl, (C1-4)alkyloxy, halogen, CF3 or cyano; Ar2 represents a 6-membered aryl ring, optionally comprising 1-3 nitrogen atoms, said ring being optionally substituted with 1-3 substituents selected from (C1-4)alkyl (optionally substituted with 1 or more halogens), (C1-4)alkyloxy (optionally substituted with 1 or more halogens), di(C1-4)alkylamino, halogen, CF3 or cyano; or a pharmaceutically acceptable salt thereof; to pharmaceutical compositions comprising the same and to the use of said 2-(benzimidazol-1-yl)-acetamide bisaryl derivatives in the treatment of TRPV1 mediated disorders.Type: GrantFiled: November 7, 2006Date of Patent: January 27, 2009Assignee: N.V. OrganonInventors: Ronald Palin, Colin Alasdair Gray
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Patent number: 7459425Abstract: The present invention generally relates to non-ethylene diamine like compounds that prevent and/or delay carbamylation of peptides.Type: GrantFiled: February 23, 2004Date of Patent: December 2, 2008Assignee: N.V. OrganonInventors: Min Wan, Phillip Ropp
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Patent number: 7435791Abstract: The present invention relates to a process for rapid solution synthesis of a peptide, the process comprising repetitive cycles of steps (a)-(d): (a) a coupling step, using an excess of an activated carboxylic component to acylate an amino component, (b) a quenching step in which a scavenger is used to remove residual activated carboxylic functions, wherein the scavenger may also be used for deprotection of the growing peptide, (c) one or more aqueous extractions and optionally, (d) a separate deprotection step, followed by one or more aqueous extractions, characterised in that the process comprises at least one step (b), referred to as step (b?), in which an amine or a thiol comprising a free anion or a latent anion is used as a scavenger of residual activated carboxylic functions. During the process of this invention the growing peptide need not be isolated until the final peptide sequence has been obtained.Type: GrantFiled: October 23, 2003Date of Patent: October 14, 2008Assignee: N.V. OrganonInventors: Ivo Franci Eggen, Paulus Bernardus Wilhelmus Ten Kortenaar, Cornelis Albert Gruson Haasnoot
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Patent number: 7435817Abstract: The present invention relates to process for the preparation of a 14-hydroxynormorphinone derivative of formula IV comprising reacting the compound of formula III, with a cobalt (II) oxidant in the presence of a mild base and air or oxygen as the cooxidant; wherein R1 is (1C-7C)alkyl optionally substituted with one or more chlorines, butenyl, vinyl, benzyl, phenyl or naphthyl; and R2 is benzyl or benzyl substituted with one or more (1C-6C)alkoxy group or benzyl substituted with one or more halogen. The process is very suitable in the production of noroxymorphone.Type: GrantFiled: August 15, 2002Date of Patent: October 14, 2008Assignee: N.V. OrganonInventors: Joannes Theodorus Maria Linders, Pieter Vrijhof
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Patent number: 7432075Abstract: 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: GrantFiled: April 3, 2007Date of Patent: October 7, 2008Assignee: N.V. OrganonInventors: Robert Van der Geize, Peter Van der Meijden, Gerda Hessels, Lubbert Dijkhuizen
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Patent number: 7396854Abstract: The present invention relates to a method of treatment of hot flushes with a 5-HT2C receptor agonist and in particular to the use of the selective 5-HT2C receptor agonists 1-[6-chloro-5-(trifluoromethyl)-2-pyridinyl]-piperazine and (S)-(+)-3-[(2,3-dihydro-5-methoxy-1H-inden-4-yl)oxy-pyrrolidine or pharmaceutically acceptable acid addition salts thereof for the manufacture of a pharmaceutical formulation adapted for the treatment of hot flushes.Type: GrantFiled: September 21, 2005Date of Patent: July 8, 2008Assignee: N.V. OrganonInventor: Hermanus Henricus Gerardus Berendsen
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Patent number: 7375106Abstract: The invention relates to a combined pharmaceutical preparation comprising an opioid diarylmethyl piperazine compounds and a NSAID. Such a preparation in which the compounds are either given sequentially or simultaneously can be used for the treatment of pain diminishing the side-effects observed in conventional opioid treatments.Type: GrantFiled: May 12, 2003Date of Patent: May 20, 2008Assignee: N.V. OrganonInventors: Andrea Houghton, Jean Cottney
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Patent number: 7375109Abstract: The present invention resides in glycine substituted thieno[2,3-d]pyrimidine derivatives according to general formula I, or a pharmaceutically acceptable salt thereof, wherein X is O or H,H A is S, NH, N(R6), O or a bond; R1 is (1-4C)alkyl, (2-4C)alkenyl, phenyl or (2-5C)heteroaryl, the phenyl or heteroaryl ring optionally being substituted with one or more of the group of substituents: hydroxy, halogen, nitro, trifluoromethyl, cyano, amino or (1-4C)(di)alkylamino and R2 is H, (1-4C)alkyl, (1-4C)alkoxy(2-4C)alkyl or hydroxy(2-4C)alkyl; R3 and R4 can be independently selected from H and hydroxy(1-4C)alkyl; R5 is H or (1-4C)alkyl; R6 can be selected from the same groups as described for R1. The compounds of the invention have LH as well as FSH receptor activating activity and can be used in fertility regulating therapies.Type: GrantFiled: August 29, 2002Date of Patent: May 20, 2008Assignee: N.V. OrganonInventors: Robert Gerardus Jules Marie Hanssen, Cornelis Marius Timmers, Jan Kelder
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Patent number: 7357046Abstract: The invention relates to a vessel for dissolution testing of a pharmaceutical delivery device, comprising: an inert vessel wall and an inert vessel bottom such that the vessel is able to hold a fluid medium; an inert retainer provided by or at the vessel wall or vessel bottom, for holding a pharmaceutical delivery device; and which retainer allows a passageway to the vessel bottom for a sampling tube. The invention further relates to a method for preparing such a vessel; a dissolution method using such a vessel and an apparatus comprising such a vessel.Type: GrantFiled: December 9, 2003Date of Patent: April 15, 2008Assignee: N. V. OrganonInventor: Rainer Kraft
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Patent number: 7354728Abstract: The invention provides a protein having an amino acid sequence as in SEQ ID 7, 8, 11 or 12, similar proteins, naturally occurring variants and homologous functional equivalents thereof, as well as the use of a polynucleotide encoding such protein, for use in an assay and for use in a method of modulation of transcriptional activity promoted by a responsive nuclear receptor and a coactivator, which coactivator is the mentioned protein and is named COASTER, and which nuclear receptor is preferrably a steroid receptor.Type: GrantFiled: August 16, 2001Date of Patent: April 8, 2008Assignee: N.V. OrganonInventors: Koen Jacob Dechering, Sietse Mosselman
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Patent number: 7345036Abstract: The present invention relates to (pyrido/thieno)-[f]-oxazepine-5-one derivatives having the general Formula (I) or a pharmaceutically acceptable salt thereof. The invention also relates to pharmaceutical compositions comprising said derivatives, and to the use of these (pyrido/thieno)-[f]-oxazepine-5-one derivatives in the treatment of neurological diseases and psychiatric disorders which are responsive to enhancement of synaptic responses mediated by AMPA receptors in the central nervous system.Type: GrantFiled: June 10, 2002Date of Patent: March 18, 2008Assignee: N.V. OrganonInventors: Simon James Anthony Grove, Julia Adam-Worall, Minggiang Zhang, Robert Gilfillan
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Patent number: 7335659Abstract: This invention provides a compound, or its possible salt, having the formula, wherein: Re and ?Re are OH, optionally independently etherified or esterified; Z is —CH2CH2— or —C(R4,R5)—, wherein R4 and R5 are independently H, (1C-2C)alkyl or form together a spiro(3C-5C)cycloalkyl; R1 is H, halogen, CF3, or (1C-4C)alkyl; R2 and R3 are independently H, halogen, —CF3, —OCF3, (1C-8C)alkyl, hydroxy, (1C-8C)alkyloxy, aryloxy, aryl(1C-8C)alkyl, halo(1C-8C)alkyl, —O(CH2)mX, wherein X is halogen or phenyl and m=2-4; —O(CH2)mNRaRb, —S(CH2)mNRaRb or —(CH2)mNRaRb, wherein m=2-4 and wherein Ra, Rb are independently (1C-8C)alkyl, (2C-8C)alkenyl, (2C-8C)alkynyl, or aryl, which alkyl, alkenyl and aryl can optionally be substituted with halogen, —CF3, —OCF3, —CN, —NO2, —OH, (1C-8C)alkoxy, aryloxy, carboxyl, (1C-8C)alkylthio, carboxylate, (1C-8C)alkyl, aryl, aryl(1C-8C)alkyl or halo(1C-8C)alkyl; or Ra and Rb form a 3-8 membered ring structure, optionally substituted with halogen, —CF3, —OCF3, —CN, —NO2, hydroxy, hydroxy(1C-Type: GrantFiled: February 14, 2003Date of Patent: February 26, 2008Assignee: N.V. OrganonInventors: Hubert Jan Jozef Loozen, Markus Wagener, Gerrit Veeneman, Eduard Willem Zwart
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Patent number: 7329510Abstract: This invention relates to a DNA sequence encoding a member of the hyperpolarized activated ion channel family (HCN) and variants thereof, and the use of said sequences in assays for the measurement of gene expression. It also relates to assays for screening of Ih activators and blockers for clinical and therapeutic use in the management of human psychiatric and neurological dysfunction in the CNS, cardiovascular dysfunction of the heart, and reproductive dysfunction and/or contraception related to Ih function in testes and spermatozoa. Further, antibodies against the expressed DNA sequences and other compounds reactive with the expressed DNA sequence are also part of the invention.Type: GrantFiled: May 22, 2001Date of Patent: February 12, 2008Assignee: N.V. OrganonInventors: John Anthony Morrow, Donald Robert Dunbar, Deborah Grace Tolan
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Patent number: 7326715Abstract: 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.Type: GrantFiled: September 21, 2006Date of Patent: February 5, 2008Assignee: N.V. OrganonInventors: Zoran Rankovic, Jiaqiang Cai
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Patent number: 7323454Abstract: The subject invention provides new progestogen esters and uses thereof.Type: GrantFiled: May 22, 2003Date of Patent: January 29, 2008Assignee: N.V. OrganonInventors: Henrik H De Nijs, Hendrikus Adrianus Antonius H.A.A. Van Der Voort, Dirk D. Leysen, Arij Jan A.J. Grootenhuis
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Patent number: 7320873Abstract: The invention describes a method to diagnose the autoimmune disease activity by detecting the presence of an autoimmune specific MHC-peptide complex in a patient suffering from an autoimmune disease. The MHC-peptide complex is associated with rheumatoid arthritis. Monoclonals antibodies to be used for this method are also described. The antibodies can also be used for therapeutic purposes.Type: GrantFiled: August 8, 2001Date of Patent: January 22, 2008Assignee: N.V. OrganonInventor: Petrus Gerardus Antonius Steenbakkers
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Patent number: 7317006Abstract: The invention relates to thieno[2,3-d]pyrimidine derivatives according to general formula I, or a pharmaceutically acceptable salt thereof, wherein N(R1)R2 are joined in a (2-6C)heterocycloalkyl ring. The compounds of the invention have LH as well as FSH receptor activating activity and can be used in fertility regulating therapies.Type: GrantFiled: August 29, 2002Date of Patent: January 8, 2008Assignee: N.V. OrganonInventors: Robert Gerard Jules Marie Hanssen, Cornelis Marius Timmers
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Patent number: 7307073Abstract: The present invention relates to benzoxazepine derivative having the general formula I, wherein X represents CO or SO2; R1, R2, R3 and R4 are independently selected from H, (C1-4)alkyl, (C1-4)alkyloxy, (C1-4)alkyloxy(C1-4)alkyl, halogen, nitro, cyano, NR8R9, NR8COR10, and CONR8R9, R5, R6 and R7 are independently H or (C1-4)alkyl; R8 and R9 are independently H or (C1-4)alkyl; or R8 and R9 form together with the nitrogen atom to which they are bound a 5- or 6-membered saturated heterocyclic ring, optionally containing a further heteroatom selected from O, S or NR11; R10 is (C1-4)alkyl; R11 is (C1-4)alkyl; A represents the residue of a 4-7 membered saturated heterocyclic ring, optionally containing an oxygen atom, the ring being optionally substituted with 1-3 substituents selected from (C1-4)alkyl, (C1-4)alkyloxy, hydroxy, halogen and oxo; or a pharmaceutically acceptable salt thereof.Type: GrantFiled: June 5, 2002Date of Patent: December 11, 2007Assignee: N.V. OrganonInventors: Simon James Anthony Grove, Mingqiang Zhang, Mohammad Shahid