Patents Assigned to N.V. Organon
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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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Publication number: 20080207598Abstract: The invention relates to indole derivative having the general Formula I wherein A represents a 5-membered aromatic heterocyclic ring, wherein X1, X2 and X3 are independently selected from N, O, S and CH; Y represents CH2, O, S or SO2; R1 is H, (C1-4)-alkyl, (C1-4)alkyloxy, CN or halogen; R2, R2?, R3, R3?, R4, R4?, R5 and R5? are independently hydrogen, (C1-4)alkyl (optionally substituted with OH) or CO—OR8; or one pair of geminal substituents R3 and R3? or R5 and R5? together represent a keto group, and the others are all hydrogen or (C1-4)alkyl; or R2 and R5 together represent a methylene or an ethylene bridge, and R2?, R3, R3?, R4, R4? and R5? are hydrogen; n is 1 or 2; R6 is H, (C1-4)alkyl (optionally substituted with OH(C1-4)alkyloxy, CO—NR9R10, CO—OR11 or 1,2,4-oxadiazol-3-yl), SO2NR12R13 or COOR14; R7 is H or halogen; R8 is (C1-4)alkyl; R9 and R10 are independently hydrogen, (C1-4)alkyl or (C3-7)cycloalkyl, the alkyl groups being optionally substituted with OH or (C1-4)alkyloxy; R11 is H or (C1-4)alType: ApplicationFiled: February 15, 2008Publication date: August 28, 2008Applicant: N.V. OrganonInventor: Julia Adam
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Publication number: 20080207571Abstract: The subject invention provides for new regimens for monophasic oral contraceptives.Type: ApplicationFiled: June 16, 2006Publication date: August 28, 2008Applicant: N.V. OrganonInventor: Victoria Jane Davis
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Publication number: 20080200671Abstract: 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.Type: ApplicationFiled: November 13, 2007Publication date: August 21, 2008Applicant: N.V. OrganonInventor: Gerhardus Johannes Heeres
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Publication number: 20080188459Abstract: This invention relates to novel amino acid derivatives of formula (I) wherein the R groups have the following meanings: —R1 is —H or -(1-4C)alkyl; —R2 is —C(O)R15 or —S(O)2R15; —R3 is —H, -(1-4C)alkyl or —OR16; —R4 is —H, -(1-4C)alkyl or —OR16; —R6 is —H or —C(R16)NOR16; —R7 is —H, -halogen, -cyano; -(1-6C)alkyl, -(2-6C)alkenyl or -(2-6C)alkynyl, all optionally substituted with -amino, -hydroxyl or -halogen; —R8 is —H, -cyano, -halogen, -nitro; -(1-6C)alkyl, -(2-6C)alkenyl, -(2-6C)alkynyl or —O(1-6C)alkyl, all optionally substituted with -amino, -hydroxyl or -halogen; -(hetero)aryl, optionally substituted with -cyano, -halogen, -(1-4C)alkyl, -(1-4C)alkoxy, -(1-4C)alkoxy(1-4C)alkyl or -(hetero)aryl; —C(R16)NOR16; —C(O)N(R17)2; —C(O)R18, —C(O)OR19, —NHC(O)R20, or —NHS(O)2R21; —R9 is —H, -halogen, -cyano, or -(1-4C)alkyl, optionally substituted with -halogen; —R10 is —H or -(1-4C)alkyl; —R11 is —H; —R12 is —H, -cyano or -(1-4C)alkyl; —R13 is —H, -(1-4C)alkyl, -halogen or -formyl; —R14 is —H, -halogen, -cyano, -(Type: ApplicationFiled: August 25, 2006Publication date: August 7, 2008Applicant: N.V. OrganonInventors: Ralf Plate, Christiaan Gerardus Johannes Maria Jans
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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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Publication number: 20080139529Abstract: The present invention relates to benzoxazepine derivative having the general formula I, wherein X represents CO or S02; 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: ApplicationFiled: October 25, 2007Publication date: June 12, 2008Applicant: N.V. OrganonInventors: Simon James Anthony Grove, Mingqiang Zhang, Mohammad Shahid
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Publication number: 20080139459Abstract: The present invention relates to conjugates of a polypeptide and an oligosaccharide, wherein the polypeptide is conjugated to at least one oligosaccharide-spacer residue, the oligosaccharide being a synthetic sulfated oligosaccharide comprising 4-18 monosaccharide units and per se having affinity to antithrombin III and the spacer being a bond or an essentially pharmacologically inactive flexible linking residue, or a pharmaceutically acceptable salt thereof. The conjugates of the invention have improved pharmacokinetic properties when compared to the original polypeptides (i.e. the corresponding non-conjugated polypeptides per se).Type: ApplicationFiled: January 31, 2006Publication date: June 12, 2008Applicant: N.V. OrganonInventors: Ebo Sybren Bos, Martin De Kort, Meertinus Jan Smit, Constant Adriaan Anton Van Boeckel
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Publication number: 20080119549Abstract: Pharmacological inhibition of fatty acid amide hydrolase (FAAH) activity leads to increased levels of fatty acid amides. Esters of alkylcarbamic acids are disclosed that are inhibitors of FAAH activity. Compounds disclosed herein inhibit FAAH activity. Described herein are processes for the preparation of esters of alkylcarbamic acid compounds, compositions that include them, and methods of use thereof.Type: ApplicationFiled: July 5, 2007Publication date: May 22, 2008Applicant: N.V. OrganonInventors: Olivier DASSE, David Putman, Timothy R. Compton, Jeff A. Parrott
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Publication number: 20080120041Abstract: The invention provides for a method for predicting potential metabolites for a compound, comprising the steps of receiving a target compound from a user applying a set of optimized reaction rules to said target compound to generate a list of potential metabolites and calculating a probability score for each product compound on said list of potential metabolites. The reaction set is optimized by starting from a starting set of reaction rules and replacing at least one reaction rule for a reaction center in said starting set of reaction rules by one, or preferably two or more new rules, which are defined to apply to a reaction of said reaction center, but now specifying or differentiating based on the structural environments of said reaction center, if at least one of said new rules has a higher probability score than the replaced reaction rule when the starting set of reaction rules and the optimized set of reaction rules are both tested with a database of known metabolites of compounds.Type: ApplicationFiled: November 12, 2007Publication date: May 22, 2008Applicant: N.V. OrganonInventors: Lars-Olaf Ridder, Markus Wagener, Johannes Petrus Maria Lommerse
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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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Publication number: 20080112892Abstract: The subject invention provides an X-ray visible drug delivery device for subdermal administration of a contraceptive or hormone replacement therapy.Type: ApplicationFiled: March 14, 2005Publication date: May 15, 2008Applicant: N.V. ORGANONInventors: Harm Veenstra, Wouter De Graaff
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Publication number: 20080107567Abstract: 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: ApplicationFiled: November 15, 2007Publication date: May 8, 2008Applicant: N.V. OrganonInventor: Rainer Kraft
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Patent number: 7369463Abstract: A timer for assisting in the control of various medical regimen is described. The timer is particularly adapted for use in avoiding or assuring conception by providing a graphic representation on the timer to alert a user as to when a medically correct step needs to be taken. The timer is provided with an alarm that alerts one as to when a transition from one particular part of, for example, a contraceptive regimen to another part of the regimen is about to occur and illustrates the transition on the graphic representation. A status of the regimen is also presented to a user. One graphic representation involves an hour-glass filled with granules corresponding in number to the amount of time left before a transition in the medical regimen is to occur.Type: GrantFiled: February 19, 2000Date of Patent: May 6, 2008Assignee: N.V. OrganonInventors: Marlies Van Dullemen, Jan Willem Bouwknegt
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Publication number: 20080102463Abstract: A nucleotide acid sequence is provided encoding a protein having NAALAdase like activity. NALADase activity has been found to be decreased in schizophrenic brain tissue. Its encoded protein can be used to screen for glutamate peptidase modulators.Type: ApplicationFiled: August 29, 2007Publication date: May 1, 2008Applicant: N.V. OrganonInventors: Colin Semple, Donald Dunbar
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Publication number: 20080093555Abstract: This invention provides a method to determine the content of water in a sample by liberating the water from the sample followed by capturing the liberated water in a gas flow and measuring cumulatively the water vapour content in the gas flow by spectroscopy, preferably frequency modulated spectroscopy.Type: ApplicationFiled: September 28, 2007Publication date: April 24, 2008Applicant: N.V. OrganonInventors: Michel Peeters, Allard Peperkamp
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Publication number: 20080089845Abstract: Described herein is a method for determining an effective dose of a composition for inhibiting fatty acid amide hydrolase activity in vivo, by first administering to a subject a dose of a test composition, and subsequently assessing if the level of a fatty acid amide in the subject increases. Also described, is a method for optimizing therapeutic efficacy for treatment of anxiety, depression, pain, or a metabolic disorder by increasing or decreasing a dose of a fatty amide hydrolase inhibitor according to a patient's fatty acid amide levels. In addition, pharmaceutical compositions are described, which contain fatty acid amide hydrolase inhibitors effective for increasing a FAA level in a patient.Type: ApplicationFiled: August 30, 2007Publication date: April 17, 2008Applicant: N.V. OrganonInventors: Timothy Compton, Jeff Parrott, Edward Monaghan, Olivier Dasse, David Putman