Patents by Inventor Raymond W. Kosley, Jr.

Raymond W. Kosley, Jr. has filed for patents to protect the following inventions. This listing includes patent applications that are pending as well as patents that have already been granted by the United States Patent and Trademark Office (USPTO).

  • Patent number: 8642603
    Abstract: The present invention relates to a series of substituted dihydro and tetrahydro oxazolopyrimidinones, specifically, to a series of 2-substituted-2,3-dihydro-oxazolo[3,2-a]pyrimidin-7-ones and 2-substituted-2,3,5,6-tetra-hydro-oxazolo[3,2-a]pyrimidin-7-ones of formula (I): Wherein p, n, X, Y, R1, R2, R3, R4, R5, R6, R7 and R8 are as defined herein. This invention also relates to methods of making these compounds including novel intermediates. The compounds of this invention are modulators of metabotropic glutamate receptors (mGluR), particularly, mGluR2 receptor. Therefore, the compounds of this invention are useful as pharmaceutical agents, especially in the treatment and/or prevention of a variety of central nervous system disorders (CNS), including but not limited to acute and chronic neurodegenerative conditions, psychoses, convulsions, anxiety, depression, migraine, pain, sleep disorders and emesis.
    Type: Grant
    Filed: September 4, 2009
    Date of Patent: February 4, 2014
    Assignee: Sanofi
    Inventors: Bin Cao, Vieroslava Gurunian, Sathapana Kongsamut, Raymond W. Kosley, Jr., Rosy Sher, Ryan E. Hartung
  • Patent number: 8283479
    Abstract: The invention relates to compounds of the formula I: in which R1, R2, X, A, B, D and Y1 to Y4 have the meanings indicated in the claims, and/or a pharmaceutically acceptable salt and/or a prodrug thereof. Because of their properties as inhibitors of chemokine receptors, especially as CXCR2 inhibitors, the compounds of the formula I and the pharmaceutically acceptable salts and prodrugs thereof are suitable for the prevention and treatment of chemokine mediated diseases.
    Type: Grant
    Filed: April 4, 2011
    Date of Patent: October 9, 2012
    Assignee: Sanofi-Aventis Deutschland GmbH
    Inventors: Stephanie Hachtel, Juergen Dedio, Holger Heitsch, Werngard Czechtizky, Sven Grueneberg, Stephen J. Shimshock, Raymond W. Kosley, Jr., Carolina L. Lanter, Hui Li, Rosy Sher, Aleksandra Weichsel
  • Publication number: 20110184177
    Abstract: The invention relates to compounds of the formula I: in which R1, R2, X, A, B, D and Y1 to Y4 have the meanings indicated in the claims, and/or a pharmaceutically acceptable salt and/or a prodrug thereof. Because of their properties as inhibitors of chemokine receptors, especially as CXCR2 inhibitors, the compounds of the formula I and the pharmaceutically acceptable salts and prodrugs thereof are suitable for the prevention and treatment of chemokine mediated diseases.
    Type: Application
    Filed: April 4, 2011
    Publication date: July 28, 2011
    Applicant: SANOFI-AVENTIS DEUTSCHLAND GMBH
    Inventors: Stephanie Hachtel, Juergen Dedio, Holger Heitsch, Werngard Czechtizky, Sven Grueneberg, Stephen J. Shimshock, Raymond W. Kosley, JR., Carolina L. Lanter, Hui Li, Rosy Sher, Aleksandra Weichsel
  • Patent number: 7919628
    Abstract: The invention relates to compounds of the formula I: in which R1, R2, X, A, B, D and Y1 to Y4 have the meanings indicated in the claims, and/or a pharmaceutically acceptable salt and/or a prodrug thereof. Because of their properties as inhibitors of chemokine receptors, especially as CXCR2 inhibitors, the compounds of the formula I and the pharmaceutically acceptable salts and prodrugs thereof are suitable for the prevention and treatment of chemokine mediated diseases.
    Type: Grant
    Filed: June 29, 2007
    Date of Patent: April 5, 2011
    Assignee: Sanofi-Aventis Deutschland GmbH
    Inventors: Stephanie Hachtel, Juergen Dedio, Holger Heitsch, Werngard Czechtizky, Sven Grueneberg, Stephen J. Shimshock, Raymond W. Kosley, Jr., Carolina L. Lanter, Hui Li, Rosy Sher, Aleksandra Weichsel
  • Patent number: 7777042
    Abstract: A composition for binding FKBP proteins is disclosed, along with a method of treating conditions associated with neuronal degeneration, wherein said composition comprises a compound of formula I, wherein, R, R1, R2, R3 and X are as defined herein.
    Type: Grant
    Filed: December 6, 2006
    Date of Patent: August 17, 2010
    Assignee: Aventis Pharmaceuticals Inc.
    Inventors: Raymond W. Kosley, Jr., Bruce Baron, Patrick Jimonet, John G. Jurcak, Stephen J. Shimshock, Xu-Yang Zhao, Rosy Sher, Paul J. Mueller, Jennifer Beall, Matthieu Barrague, Joseph W. Guiles
  • Publication number: 20100075994
    Abstract: The present invention relates to a series of substituted dihydro and tetrahydro oxazolopyrimidinones, specifically, to a series of 2-substituted-2,3-dihydro-oxazolo[3,2-a]pyrimidin-7-ones and 2-substituted-2,3,5,6-tetra-hydro-oxazolo[3,2-a]pyrimidin-7-ones of formula (I): Wherein p, n, X, Y, R1, R2, R3, R4, R5, R6, R7 and R8 are as defined herein. This invention also relates to methods of making these compounds including novel intermediates. The compounds of this invention are modulators of metabotropic glutamate receptors (mGluR), particularly, mGluR2 receptor. Therefore, the compounds of this invention are useful as pharmaceutical agents, especially in the treatment and/or prevention of a variety of central nervous system disorders (CNS), including but not limited to acute and chronic neurodegenerative conditions, psychoses, convulsions, anxiety, depression, migraine, pain, sleep disorders and emesis.
    Type: Application
    Filed: September 4, 2009
    Publication date: March 25, 2010
    Applicant: SANOFI-AVENTIS
    Inventors: Bin CAO, Vieroslava GURUNIAN, Sathapana KONGSAMUT, Raymond W. KOSLEY, JR., Rosy SHER, Ryan E. HARTUNG
  • Patent number: 7125903
    Abstract: The compounds are of the class thienoisoxazolyl- and thienylpyrrazolyl-phenoxy substituted propyl derivatives, useful as D4 antagonists. Said compounds are useful for the treatment of medical conditions mediated by inhibition of D4 receptor. These conditions comprise, for example, Attention Deficit Hyperactivity Disorder, Obsessive-Compulsive Disorder, Psychoses, Substance Abuse, Substance Dependence, Parkinson's Disease, Parkinsonism, Tardive Diskinesia, Gilles de la Tourette Syndrome, Conduct Disorder, and Oppositional Defiant Disorder. A further aspect of the invention is to provide a pharmaceutical composition, intermediates, and a method of making said class of compounds.
    Type: Grant
    Filed: September 13, 2000
    Date of Patent: October 24, 2006
    Assignee: Aventis Pharmaceuticals Inc.
    Inventors: David M. Fink, Brian S. Freed, Nicholas J. Hrib, Raymond W. Kosley, Jr., George E. Lee, Gregory H. Merriman, Barbara S. Rauckman
  • Patent number: 6479495
    Abstract: Novel aminoalkylphenols, intermediates and processes for the preparation thereof, and methods of relieving memory dysfunction utilizing the aminoalkylphenols or compositions thereof are disclosed.
    Type: Grant
    Filed: December 10, 1999
    Date of Patent: November 12, 2002
    Assignee: Aventis Pharmaceuticals Inc.
    Inventors: Raymond W. Kosley, Jr., Mark G. Palermo, Stephen J. Shimshock, Veronica Wolf
  • Patent number: 6413986
    Abstract: Novel [[(aminocarbonyloxy)-1-indan]-2-yl]methylpiperidines of the formula wherein R is hydrogen, loweralkyl, or a group of the formula R1 is hydrogen or a group of the formula W, X and Y are hydrogen, loweralkyl, loweralkoxy, halogen, nitrogen, or trifluoromethyl; n is 1 or 2; the pharmaceutically acceptable acid addition salts thereof intermediates of the formula and process for the preparation thereof, and a method of relieving memory dysfunction, employing compounds and compositions thereof are disclosed.
    Type: Grant
    Filed: May 8, 1995
    Date of Patent: July 2, 2002
    Assignee: Aventis Pharmaceuticals Inc.
    Inventors: Raymond W. Kosley, Jr., Bettina Spahl, Richard C. Effland
  • Patent number: 6323195
    Abstract: This application relates to compounds of the formula wherein R1 is hydrogen, (C1-C12alkylcarbonyl, (C1-C12)alkoxycarbonyl, mono(C1-C12)alkylaminocarbonyl, or di(C1-C12)alkylaminocarbonyl; R2 is hydrogen, (C3-C12)alkenylcarbonyloxy, (C3-C12)cycloalkylcarbonyloxy, (C3-C12)cycloalkyl(C1-C12)alkylcarbonyloxy, oxygen containing heterocycloxy, oxygen containing heterocyclylcarbonyloxy, sulfur containing heterocyclyloxy, sulfur containing heterocyclylcarbonyloxy, nitrogen containing hetercyclyloxy, nitrogen containing heterocyclylcarbonyloxy, haloalkylsulfonyloxy, (C1-C6)alkylsilyloxy; R3 is hydrogen, halo or (C1-C4)alkyl; R4 is hydrogen or (C1-C6)alkyl; with the proviso that R1 and R2 are not both hydrogen when R3 and R4 are hydrogen; all geometric, and optical stereoisomers thereof, or a pharmaceutically acceptable addition salt thereof; which compounds are useful for the treatment of memory dysfunction characterized by decreased cholinergic function, pharmaceutical compositions containing t
    Type: Grant
    Filed: October 15, 1993
    Date of Patent: November 27, 2001
    Assignee: Aventis Pharmaceuticals Inc.
    Inventors: Raymond W. Kosley, Jr., Larry Davis, Veronica Taberna
  • Patent number: 6323196
    Abstract: This application relates to compounds of the formula wherein R1 is hydrogen, (C1-C12)alkylcarbonyl, (C1-C12)alkoxycarbonyl, mono(C1-C12)alkylaminocarbonyl, or di(C1-C12)alkylaminocarbonyl; R2 is mono(C1-C18)alkylaminocarbonyloxy, di(C1-C8)alkylaminocarbonyloxy, or aryl(C1-C4)alkylaminocarbonyloxy; R3 is hydrogen or halo; or a pharmaceutically acceptable acid addition salt thereof, which compounds are useful for the treatment of memory dysfunction characterized by decreased cholinergic function, pharmaceutical compositions containing the compounds and methods for making and using the compounds.
    Type: Grant
    Filed: October 15, 1993
    Date of Patent: November 27, 2001
    Assignee: Aventis Pharmaceuticals Inc.
    Inventors: Raymond W. Kosley, Jr., Larry Davis, Veronica Taberna
  • Patent number: 6316439
    Abstract: This application relates to compounds of the formula wherein R1 is hydrogen, (C1-C12)alkylcarbonyl, (C1-C12)alkoxycarbonyl, aryl(C1-C12)alkylaminocarbonyl, mono(C1-C18)alkylaminocarbonyl or di(C1-C8)alkylaminocarbonyl; R2 is (C1-C12)alkylcarbonyloxy, aryl(C1-C4)alkylcarbonyloxy, (C1-C12)alkoxycarbonyloxy, arylcarbonyloxy, hydroxy, (C1-C6)alkoxycarbonyl(C1-C6)alkoxy or hydroxy(C1-C10)alkoxy; R3 is hydrogen or halo; and pharmaceutically acceptable addition salts; with the proviso that when R2 is hydroxy, R1 and R3 are not both hydrogen or when R2 is hydroxy and R3 is hydrogen, R1 is not methylcarbonyl; which compounds are useful for the treatment of memory dysfunction characterized by decreased cholinergic function, pharmaceutical compositions containing the compounds and methods for making and using the compounds.
    Type: Grant
    Filed: October 15, 1993
    Date of Patent: November 13, 2001
    Assignee: Aventis Pharamaceuticals Inc.
    Inventors: Raymond W. Kosley, Jr., Larry Davis, Veronica Taberna
  • Patent number: 6063793
    Abstract: The present invention is directed to esters of (+)-.alpha.-(2,3-Dimethoxyphenyl)-1-[2-(4-fluorophenyl)ethyl]-4-piperidine methanol, pharmaceutical formulations, methods of making and methods of using these esters. These compounds antagonize the effects of serotonin at the 5HT.sub.2A receptor and are useful in treating various conditions such as, for example, psychoses such as schizophrenia.
    Type: Grant
    Filed: June 22, 1999
    Date of Patent: May 16, 2000
    Assignee: Hoechst Marion Roussel, Inc.
    Inventors: Albert A. Carr, Raymond W. Kosley, Jr., Luc Van Hijfte
  • Patent number: 6028083
    Abstract: The present invention is directed to esters of (+)-.alpha.-(2,3 Dimethoxyphenyl)-1-[2-(4-fluorophenyl)ethyl]-4-piperidinemethanol, pharmaceutical formulations, methods of making and methods of using these esters. These compounds antagonize the effects of serotonin at the 5HT.sub.2A receptor and are useful in treating various conditions such as, for example, psychoses such as schizophrenia.
    Type: Grant
    Filed: July 25, 1997
    Date of Patent: February 22, 2000
    Assignee: Hoechst Marion Roussel, Inc.
    Inventors: Albert A. Carr, Raymond W. Kosley, Jr., Luc Van Hijfte
  • Patent number: 5869520
    Abstract: Novel carbamoyloxylabdanes, intermediates and processes for the preparation thereof, and methods for reducing intraocular pressure and treating cardiac failure utilizing compounds and compositions thereof are disclosed.
    Type: Grant
    Filed: January 8, 1997
    Date of Patent: February 9, 1999
    Assignee: Hoechst Marion Roussel, Inc.
    Inventors: Raymond W. Kosley, Jr., Robert Joseph Cherill, Gerard O'Malley
  • Patent number: 5847167
    Abstract: Novel carbamoyloxylabdanes, intermediates and processes for the preparation thereof, and methods for reducing intraocular pressure and treating cardiac failure utilizing compounds and compositions thereof are disclosed.
    Type: Grant
    Filed: June 30, 1997
    Date of Patent: December 8, 1998
    Assignee: Hoechst Marion Roussel, Inc.
    Inventors: Raymond W. Kosley, Jr., Robert Joseph Cherill, Gerard O'Malley
  • Patent number: 5777108
    Abstract: This application relates to compounds of the formula ##STR1## wherein R.sup.1, R.sup.2, R.sup.3 and R.sup.4 are defined within, which compounds are useful for the treatment of memory dysfunction characterized by decreased cholinergic function, pharmaceutical compositions containing the compounds and methods for making and using the compounds.
    Type: Grant
    Filed: May 22, 1995
    Date of Patent: July 7, 1998
    Assignee: Hoechst Marion Roussel, Inc.
    Inventors: Raymond W. Kosley, Jr., Larry Davis, Veronica Taberna
  • Patent number: 5646300
    Abstract: There are disclosed neuroprotective compounds having the formula ##STR1## wherein the moieties are defined in the specification, and processes for making them.
    Type: Grant
    Filed: June 1, 1995
    Date of Patent: July 8, 1997
    Assignee: Hoechst Marion Roussel, Inc.
    Inventors: Raymond W. Kosley, Jr., Denise M. Flanagan, Lawrence L. Martin, Peter A. Nemoto
  • Patent number: 5646175
    Abstract: Novel carbamoyloxylabdanes, intermediates and processes for the preparation thereof, and methods for reducing intraocular pressure and treating cardiac failure utilizing compounds and compositions thereof are disclosed.
    Type: Grant
    Filed: June 1, 1995
    Date of Patent: July 8, 1997
    Assignee: Hoechst Marion Roussel, Inc.
    Inventors: Raymond W. Kosley, Jr., Robert Joseph Cherill, Gerard O'Malley
  • Patent number: 5605925
    Abstract: There are disclosed 1-aminoacetamidopyrroles and 1-amino-2-(substituted)pyrroles and related compounds of the formula ##STR1## wherein all substituents are defined herein, which are useful as glycine partial agonists and for the enhancement of learning and memory and for the treatment of memory dysfunctions associated with neurodegenerative disorders and are thus indicated in the treatment of Alzheimer's disease and other senile dementias.
    Type: Grant
    Filed: November 7, 1994
    Date of Patent: February 25, 1997
    Assignee: Hoechst Marion Roussel, Inc.
    Inventors: Lawrence L. Martin, Raymond W. Kosley, Jr., Denise M. Flanagan, Gert U. Kuerzel, Peter A. Nemoto, David G. Wettlaufer