Patents Assigned to N.V. Organon
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Patent number: 7910756Abstract: The invention provides a process for the preparation of 2-substituted-derivatives of estrone and estradiol. The invention also provides several novel compounds, which can be intermediates in the process, and processes to prepare these novel compounds. The invention also provides 2-alkoxy-estrone, 2-alkoxy-estradiol or mixtures thereof essentially free from other estrogenic intermediates.Type: GrantFiled: August 1, 2005Date of Patent: March 22, 2011Assignee: N.V. OrganonInventors: Johannes Stoelwinder, Nicolaas Elisabeth Cornelis Moers
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Publication number: 20110065764Abstract: The present invention relates to isoxazole-3-carboxamide derivative having the general Formula (I), or a pharmaceutically acceptable salt thereof, to pharmaceutical compositions comprising the same, as well as to the use of said isoxazole-3-carboxamide derivatives for the treatment of TRPV1 mediated disorders, such as acute and chronic pain disorders, acute and chronic neuropathic pain, acute and chronic inflammatory pain, respiratory diseases, and lower urinary tract disorders.Type: ApplicationFiled: July 31, 2008Publication date: March 17, 2011Applicant: N.V. ORGANON AND PHARMACOPEIA, LLCInventors: Andrew Laird Roughton, Koc-Kan Ho, Michael Ohlmeyer, Irina Neagu, Steven G. Kultgen, Nasrin Ansari, Yajing Rong, Paul David Ratcliffe, Ronald Palin
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Patent number: 7906504Abstract: Disclosed herein are 2-(1-oxo-1H-isoquinolin-2-yl)acetamide derivative 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 2-(1-oxo-1H-isoquinolin-2-yl)acetamide derivatives according to the present invention and their use in therapy.Type: GrantFiled: September 10, 2007Date of Patent: March 15, 2011Assignee: N.V. OrganonInventors: Jeffrey Letourneau, Jui-Hsiang Chan, Patrick Jokiel, Michael Ohlmeyer, Irina Neagu, Christopher Riviello, John Richard Morphy, Susan Elizabeth Napier, Koc-Kan Ho
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Patent number: 7893088Abstract: The present invention relates to 6-substituted isoquinoline derivatives having the general Formula I wherein X is O, S or NH; Y is OH or NH2; m is 0, 1 or 2; n is 0 or 1; o is 0 or 1; R1 is H, when Y is NH2; or R1 is H, (C1-4)alkyl or halogen, when Y is OH; R2 and R3 are independently H, (C1-4)alkyl or halogen; R4 is H or (C1-6)alkyl, optionally substituted with halogen, (C3-7)cycloalkyl, (C6-10)aryl or a saturated 5- or 6-membered heterocyclic ring comprising 1-3 heteroatoms independently selected from O, S and N, the (C6-10)aryl and heterocyclic ring being optionally substituted with (C1-4)alkyl, (C1-4)alkyloxy or halogen; R5 is H or (C1-4)alkyl; or a pharmaceutically acceptable salt thereof, with the proviso that the compounds of Formula I wherein X is O, Y is OH , n is 0 and m+o=2 are excluded, to pharmaceutical compositions comprising the same, as well as to the use of said 6-substituted isoquinoline derivatives for the preparation of a medicament for the treatment of ROCK-I related disorders such asType: GrantFiled: August 16, 2007Date of Patent: February 22, 2011Assignee: N.V. OrganonInventors: Peter Christopher Ray, Steven Laats, John Richard Morphy, Brad Sherborne
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Publication number: 20110039832Abstract: The invention relates to 5,6-dihydropyrrolo[2,1-a]isoquinoline and pyrrolo[2,1-a]isoquinoline derivatives according to general formula (I) or a pharmaceutically acceptable salt thereof. The compounds can be used for the treatment of infertility.Type: ApplicationFiled: February 6, 2009Publication date: February 17, 2011Applicant: N.V. OrganonInventors: Rachel Deborah van Rijn, Hubert Jan Josef Loozen, Cornelis Marius Timmers, Lar Anders van der Veen, Willem Frederik Johan Karstens
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Patent number: 7888394Abstract: Pharmacological inhibition of fatty acid amide hydrolase (FAAH) activity leads to increased levels of fatty acid amides. The alkylcarbamic acid aryl ester of Formula (I), KDS-4103, is a FAAH inhibitor. Described herein is a process for the preparation of the compound of Formula (I), characterization of polymorphs of the FAAH inhibitor, and their uses therof.Type: GrantFiled: August 16, 2007Date of Patent: February 15, 2011Assignee: N.V. OrganonInventors: David Putman, Olivier Dasse
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Publication number: 20110030681Abstract: A dispenser for administering a pharmaceutical substance in the form of a plurality of separate unit doses of the substance, comprising a housing, an actuator, a delivery outlet for administering at least one unit dose at a time, a transport mechanism for bringing the unit doses sequentially in operative association with the delivery outlet and a delaying arrangement to impose a lockout interval between administering sequential dosesType: ApplicationFiled: April 17, 2007Publication date: February 10, 2011Applicant: N.V. ORGANONInventors: Karin DE VRIES, Wim JANSEN
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Publication number: 20110028451Abstract: The invention relates to benzoindazole derivatives according to general Formula I or a pharmaceutically acceptable salt thereof. The compounds can be used for the treatment of infertility.Type: ApplicationFiled: July 29, 2010Publication date: February 3, 2011Applicant: N.V. OrganonInventors: Cornelis Marius Timmers, Hubert Jan Jozef Loozen
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Publication number: 20110028450Abstract: The invention relates to ring-annulated dihydropyrrolo[2,1-a]isoquinoline compounds according to general Formula I or a pharmaceutically acceptable salt thereof. The compounds can be used for the treatment of infertility.Type: ApplicationFiled: July 27, 2010Publication date: February 3, 2011Applicant: N.V. OrganonInventors: Cornelis Marius Timmers, Hubert Jan Jozef Loozen, Herman Thijs Stock
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Publication number: 20110020177Abstract: A mixing apparatus (1) for mixing slaughter offal with a preservative agent, the apparatus comprising an offal collection tank (3) with a bottom (4) provided with a discharge opening (5) connectable to a closable discharge, an agitator (8) extending into the offal collection tank, and a pump unit (9) operatively connectable to the discharge, wherein the apparatus further comprises a preservative reservoir (7) mounted on top of the collection tank (3). A collection and preservation system is provided, wherein the addition of preservation agent can be strictly controlled, can easily and quickly be installed and connected when it is to be used. After use, the system is easily removed and cleaned.Type: ApplicationFiled: July 22, 2010Publication date: January 27, 2011Applicant: N. V. OrganonInventors: Adolph Bartholomeus Gijtenbeek, Harry van Tuijn, Marinus Johannes Gerardus Maria Ploegmakers
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Patent number: 7872147Abstract: Disclosed are novel amino acid derivatives of formula (I) and (II) processes for the preparation thereof, and their use in the preparation of trans-5-chloro-2-methyl-2,3,3a,12b-tetrahydro-1H-dibenz[2,3:6,7]oxepino-[4,5-c]pyrrole.Type: GrantFiled: April 6, 2006Date of Patent: January 18, 2011Assignee: N. V. OrganonInventors: Gerardus Johannes Kemperman, Jacobus Johannes Maria Van Der Linden, Michael R. Reeder
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Publication number: 20110009428Abstract: The compounds of the subject invention have a structure according to formula I: wherein X is S or SO2; R1 is (1C-6C)alkyl, (3C-6C)alkenyl, or (3C-6C)alkynyl, each optionally substituted with (3C-6C)cycloalkyl, OH, OC(O)(1C-4C)alkyl, (1C-4C)alkoxy, halogen, cyano, formyl, C(O)(1C-4C)alkyl, CO2H, CO2(1C-4C)alkyl, C(O)NR5R6, S(O)(1C-4C)alkyl or S(O)2(1C-4C)alkyl; R2 is hydrogen, (1C-4C)alkyl or C(O)(1C-4C)alkyl; R3 is a phenyl group optionally substituted with (1C-4C)alkyl, (1C-4C)fluoroalkyl, (1C-4C)alkoxy, (1C-4C)fluoroalkoxy, halogen, cyano or nitro; or R3 is a 5- or 6-membered aromatic heterocyclic ring structure optionally substituted with (1C-4C)alkyl, (1C-4C)fluoroalkyl, (1C-4C)alkoxy, halogen or cyano; R4 is a phenyl group or an aromatic 6-membered heterocycle, substituted at the ortho position with 1-hydroxy(1C-4C)alkyl, (1C-4C)alkoxy, C(O)(1C-4C)alkyl, CO2(1C-4C)alkyl, C(O)NH2, cyano, nitro, or CH?NOR7, and optionally further substituted with (1C-2C)alkyl, (1C-2C)fluoroalkyl or halogen; or R4Type: ApplicationFiled: September 22, 2010Publication date: January 13, 2011Applicant: N.V. OrganonInventors: Jaap Van Der Louw, Neeltje Miranda Teerhuis, Johannes Petrus Maria Lommerse, Herman Thijs Stock, Pedro Harold Han Hermkens
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Patent number: 7868017Abstract: 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: GrantFiled: September 29, 2006Date of Patent: January 11, 2011Assignee: N.V. OrganonInventors: Susan Elizabeth Napier, Matilda Jane Bingham, Margaret Jean Huggett, Mark Huggett, Yasuko Kiyoi, Olaf Nimz
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Patent number: 7868193Abstract: 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 1-3 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.Type: GrantFiled: May 1, 2001Date of Patent: January 11, 2011Assignee: N.V. OrganonInventor: Hubert Jan Jozef Loozen
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Publication number: 20110003976Abstract: During the production of recombinant proteins from gram negative bacteria, lipopolysaccharides (LPS, endotoxin) are released along with the protein of interest. In many instances, LPS will copurify with the target protein due to specific or non-specific protein-ILPS interactions. We have investigated the ability of alkanediols to effect the separation of LPS from protein-LPS complexes while the complexes are immobilized on anion or cation exchange chromatographic media. Alkanediols provide a safer alternative to the use of other organics such as alcohols or acetonitrile due to their lower toxicity and decreased flammability. In addition, they are less costly than many of the detergents that have been used for such purposes. LPS removal efficiency increased with increasing alkane chain length. 1,2-alkanediols were more effective than terminal alkanediols in the separation of LPS from protein LPS complexes.Type: ApplicationFiled: May 19, 2010Publication date: January 6, 2011Applicant: N.V. OrganonInventors: Philip Alfred Ropp, Michael Van Alen Murray
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Publication number: 20100331292Abstract: The present invention relates to substituted steroid compounds having the formula Wherein R1 is H or halogen; R2 is H, (1C-4C)alkyl, (1C-4C)acyl, glucuronyl or sulfamoyl; R3 is H or halogen; R4 is H, (1C-4C)alkyl, (2C-4C)alkenyl or (2C-4C)alkynyl; R5 is methyl or ethyl; R6 is H or methyl; R7 is H or methyl; R8 is H or acyl for use in the treatment and prevention of endometriosis, for contraception, for hormonal therapy in perimenopausal and post-menopausal women, for the treatment of osteoporosis and for the treatment uterine fibroids and other menstrual-related disorders, such as dysfunctional uterine bleeding.Type: ApplicationFiled: June 8, 2010Publication date: December 30, 2010Applicant: N.V. OrganonInventors: Fredericus Antonius Dijcks, Hubert Jan Jozef Loozen, Samira Addo, Antonius Gerardus Hendrikus Ederveen
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Patent number: 7858794Abstract: The present invention relates to tetrahydroquinoline derivatives having gene formula (I) or a pharmaceutically acceptable salt thereof, wherein R1 and R2 are H or Me; R3 is H, hydroxy, (1-4C)alkoxy, (di)(1-4C)alkylamino(2-4C)alkoxy or (2-6)heterocycloakl(2-4C)alkoxy; R4 is H, OH, (1-4C)alkoxy or R7; R5 is H, OH, (1-4C)alkoxy or R7, with the proviso that if R4 is H, R5 is not H, OH or (1-4C)alkoxy and that if R5 is H, R4 is not H, OH or (1-4C)alkoxy; R6 is (2-5C)heteroaryl, (6C)aryl, (3-8C)cycloalkyl, (2 6C)heterocycloalkyl or (1-6C)alkyl; R7 is amino, (di)(1-4C)alkylamino, (6C)arylcarbonylamino, (6C)arylcarbonyloxy, (2-5C) heteroarylcarbonylamino, (2-5C)heteroarylcarbonyloxy, R8-(2-4C)alkylamino, R8-(2-4C)alkoxy, R9-methylamino or R9-methoxy; R8 is hydroxy, amino, (-14C)alkoxy, (di)(1-4C)alkylamino, (2-6C)heterocycloalkyl, (2-6C) heterocycloalkylcarbonylamino, (di)(1-4C)alkylaminocarbonylamino, (1-4C)alkoxycarbonylamino and R9 is aminocarbonyl, (di)(1-4C)alkylaminocarbonyl, (2-5C)heteroaryl or (6C)aryl.Type: GrantFiled: December 16, 2003Date of Patent: December 28, 2010Assignee: N.V. OrganonInventors: Cornelis Marius Timmers, Willem Frederik Karstens
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Publication number: 20100324021Abstract: The invention relates to imidazoiso[5,1-a]quinoline and 5,6-dihydro-imidazoiso[5,1-a]quinoline derivatives according to general Formula I or a pharmaceutically acceptable salt thereof. The compounds can be used for the treatment of infertility.Type: ApplicationFiled: May 25, 2010Publication date: December 23, 2010Applicant: N.V. OrganonInventors: Hubert Jan Jozef Loozen, Cornelius Marius Timmers
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Patent number: 7846966Abstract: The invention provides chroman compounds having formula 1 wherein R1 is (1C-4C)alkyl, (2C-4C)alkenyl or (2C-4C)alkynyl, and independently R1 has a cis-orientation in relation to the exocyclic phenyl group at the 2-position of the skeleton; R4 is H, Hal, CF3, OH or (1C-2C)alkyloxy; R2, R3, and R5 are independently H, Hal, CF3, (1C-4C)alkyl, (2C-4C)alkenyl or (2C-4C)alkynyl and prodrugs thereof for the manufacture of a medicine for estrogen-receptor related treatments.Type: GrantFiled: May 8, 2009Date of Patent: December 7, 2010Assignee: N.V. OrganonInventors: Gerrit Herman Veeneman, Neeltje Miranda Teerhuis
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Patent number: 7838516Abstract: The invention provides 15?-substituted steroidal compounds having selective estrogen receptor activity according to Formula I: wherein, R1 is H, C1-5 alkyl, C1-12 acyl, di-(C1-5 alkyl)aminocarbonyl, (C1-5alkyl)oxycarbonyl or sulfamoyl, R2 is H, C1-3 alkyl, C2-3 alkenyl or C2-3 alkynyl, each of which may be optionally substituted with a halogen, R3 is C1-2 alkyl, ethenyl or ethynyl, each of which may be optionally substituted with a halogen, and R4 is H or C1-12 acyl.Type: GrantFiled: September 5, 2005Date of Patent: November 23, 2010Assignee: N.V. OrganonInventors: Hubert Jan Jozef Loozen, Antonius Gerardus Hendrikus Ederveen, Fredericus Antonius Dijcks