Patents Represented by Attorney, Agent or Law Firm Susan L. Hess
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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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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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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: 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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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
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Patent number: 7838518Abstract: 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: GrantFiled: February 5, 2003Date of Patent: November 23, 2010Assignee: N.V. OrganonInventors: Daniel Spinks, Richard E. Armer, David J. Miller, Zoran Rankovic, Gayle Spinks, Jordi Mestres, David Robert Jaap
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Patent number: 7820649Abstract: 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: GrantFiled: September 10, 2007Date of Patent: October 26, 2010Assignee: N.V. OrganonInventors: Jeffrey Letourneau, Patrick Jokiel, Susan Elizabeth Napier, Koc-Kan Ho, Michael Ohlmeyer, Duncan Robert McArthur, Fiona Jeremiah, Paul David Ratcliffe, Jurgen Schulz
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Patent number: 7820707Abstract: 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: GrantFiled: June 29, 2007Date of Patent: October 26, 2010Assignee: N.V. OrganonInventors: Kevin James Gillen, Craig Jamieson, John Kinnaird Ferguson MacLean, Elizabeth Margaret Moir, Zoran Rankovic
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Patent number: 7812036Abstract: 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: GrantFiled: April 21, 2005Date of Patent: October 12, 2010Assignee: 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: 7807686Abstract: 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: GrantFiled: March 10, 2006Date of Patent: October 5, 2010Assignee: N.V. OrganonInventors: Jeffrey Letourneau, Christopher Riviello, Koc-Kan Hoc, Jui-Hsiang Chan, Michael Ohlmeyer, Patrick Jokiel, Irina Neagu, John Richard Morphy, Susan Elizabeth Napier
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Patent number: 7795280Abstract: 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: GrantFiled: November 3, 2003Date of Patent: September 14, 2010Assignee: N.V. OrganonInventors: Pedro Harold Han Hermkens, Herman Thijs Stock, Jaap Van Der Louw, Neeltje Miranda Teerhuis, Johannes Petrus Maria Lommerse
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Patent number: 7763732Abstract: 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: GrantFiled: August 18, 2006Date of Patent: July 27, 2010Assignee: N.V. OrganonInventors: Paul David Ratcliffe, Julia Adam-Worrall, Angus John Morrison, Stuart John Francis, Takao Kiyoi
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Patent number: 7737136Abstract: 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: GrantFiled: April 1, 2003Date of Patent: June 15, 2010Assignee: N.V. OrganonInventors: Pedro Harold Han Hermkens, Hans Lucas, Paul Peter Marie Antonius Dols, Johannes Bernardus Maria Rewinkel, Brigitte Johanna Bernita Folmer
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Patent number: 7051906Abstract: The invention provides a pharmaceutical package including a polypropylene bottle in which is disposed a solution containing a pharmaceutical product, where the solution does not fill the bottle completely and some air is disposed in the bottle, and where the package, after autoclaving at at least 121C and for at least 20 minutes, suffers no deformation, does not shrink, and does not explode, and where the package retains a sufficiently high squeezability to dispense the solution.Type: GrantFiled: October 9, 2001Date of Patent: May 30, 2006Assignee: Novartis AGInventors: Gyorgy Lajos Kis, Eckhard Krautler
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Patent number: 6777429Abstract: The present invention is related to an ophthalmic composition comprising ketotifen as a pharmaceutically active agent.Type: GrantFiled: July 19, 2000Date of Patent: August 17, 2004Assignee: Novartis AGInventors: Marcia Johanna Adam, Andrea Fetz, Gyorgy Lajos Kis
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Patent number: 6774137Abstract: The present invention is related to an ophthalmic composition comprising ketotifen as a pharmaceutically active agent.Type: GrantFiled: April 29, 2002Date of Patent: August 10, 2004Assignee: Novartis AGInventors: Marcia Johanna Adam, Andrea Fetz, Gyorgy Lajos Kis
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Patent number: 6670379Abstract: Compounds of formula (I) in free or salt form, where Ar1 is phenyl substituted by one or more halogen atoms, Ar2 is phenyl or naphthyl which is unsubstituted or substituted by one or more substituents selected from halogen, cyano, hydroxy, nitro, C1-C8-alkyl, C1-C8-haloalkyl, C1-C8-alkoxy or C1-C8-alkoxycarbonyl, R1 is hydrogen or C1-C8-alkyl optionally substituted by hydroxy, C1-C8-alkoxy, acyloxy, N(R2)R3, halogen, carboxy, C1-C8-alkoxycarbonyl, —CON(R4)R5 or by a monovalent cyclic organic group, R2 and R3 are each independently hydrogen or C1-C8-alkyl, or R2 is hydrogen and R3 is acyl or —SO2R6, or R2 and R3 together with the nitrogen atom to which they are attached denote a 5 or 6-membered heterocyclic group, R4 and R5 are each independently hydrogen or C1-C8-alkyl, or R4 and R5 together with the nitrogen atom to which they are attached denote a 5 or 6-membered heterocyclic group, R6 is C1-C8-alkyl, C1-C8-haloalkyl, or phenyl optionally substituted by C1-C8-alkyl, and n is 1,Type: GrantFiled: April 17, 2003Date of Patent: December 30, 2003Assignee: Novartis AGInventors: Trevor John Howe, Gurdip Bhalay, Darren Mark Le Grand, Thomas Storz
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Patent number: 6288275Abstract: Carboxylic acids, particularly dicarboxylic acids, are separated from a fermentation broth by adjusting the pH of the fermentation broth to about 2.0 or below, and then heating the broth to a temperature sufficient to cause formation of three immiscible phases, one of which is an organic phase containing the carboxylic acids.Type: GrantFiled: July 9, 1999Date of Patent: September 11, 2001Assignee: Henkel CorporationInventor: Stephen W. Turner
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Patent number: 6187903Abstract: A dimeric fatty acid and/or dimeric fatty ester product having a low residual content of interesters is obtained by hydrolyzing the interesters to provide monomeric unsaturated fatty acids and alcohols as the hydrolysates and thereafter removing the hydrolysates from the dimeric fatty acid and/or dimeric fatty ester product.Type: GrantFiled: July 29, 1999Date of Patent: February 13, 2001Assignee: Cognis CorporationInventors: A. Fred Elsasser, Laura A. McCargar