Jennifer Quyen Tran

6372743, Apr 16, 2002

Sep 29, 2000

09/676970

James W. Darrow - Wallingford CT
Stephane De Lombaert - Madison CT
Charles Blum - Westbrook CT
Jennifer Tran - Guilford CT
Mark Giangiordano - Branford CT
David Andrew Griffith - Old Saybrook CT
Philip Albert Carpino - Groton CT

Neurogen Corporation - Branford CT
Pfizer Inc. - New York NY

A61K 3153

514246, 514245, 514258, 544194, 544197, 544198, 544204, 544206, 544209, 544211, 544212, 544263, 544281

Disclosed are compounds of the formula: where R , R , R , R , R , R , and X are defined herein. These compounds are selective modulators of NPY1 receptors. These compounds are useful in the treatment of a number of CNS disorders, metabolic disorders, and peripheral disorders, particularly eating disorders and hypertension. Methods of treatment of such disorders and well as packaged pharmaceutical compositions are also provided. Compounds of the invention are also useful as probes for the localization of NPY1 receptors and as standards in assays for NPY1 receptor binding. Methods of using the compounds in receptor localization studies are given.

6444819, Sep 3, 2002

Oct 11, 2001

09/975535

Renata Xavier Kover - New Haven CT
Salva Terdjanian - New Britain CT
Jennifer Tran - Branford CT
Andrew Thurkauf - Danbury CT

Neurogen Corporation - Branford CT

C07D22120

546 18, 548411, 548216, 548152, 544 6, 544 70, 540466, 540543

Disclosed are compounds of the formula: or pharmaceutically acceptable addition salts thereof wherein: Y represents oxygen or sulfur; Z is nitrogen or CH; R , R and R independently represent organic or inorganic substituents; R and R â independently represent hydrogen, alkyl or form a ring with the atom to which they are attached; R represents hydrogen, alkyl, alkoxy, or alkylthio, and R represents hydrogen or alkyl; or R and R form a ring together with the atoms to which they are attached; and R , R , R , R , and R independently represent hydrogen or alkyl, which compounds are useful for the treatment and/or prevention of neuropsychological disorders including, but not limited to, schizophrenia, mania, dementia, depression, anxiety, compulsive behavior, substance abuse, Parkinson-like motor disorders and motion disorders related to the use of neuroleptic agents.

6476038, Nov 5, 2002

Sep 29, 2000

09/676972

James W. Darrow - Wallingford CT
Charles Blum - Westbrook CT
Jennifer Tran - Guilford CT
Mark Giangiordano - Branford CT
David Andrew Griffith - Old Saybrook CT
Philip Albert Carpino - Groton CT

Neurogen Corporation - Branford CT
Pfizer Inc. - New York NY

C07D48704

514258, 544281

Disclosed are compounds of the formula: where R , R , R , R , R , R , and X are defined herein. These compounds are selective modulators of NPY1 receptors. These compounds are useful in the treatment of a number of CNS disorders, metabolic disorders, and peripheral disorders, particularly eating disorders and hypertension. Methods of treatment of such disorders and well as packaged pharmaceutical compositions are also provided. Compounds of the invention are also useful as probes for the localization of NPY1 receptors and as standards in assays for NPY1 receptor binding. Methods of using the compounds in receptor localization studies are given.

6486164, Nov 26, 2002

Dec 20, 2001

10/027150

Jennifer N. Tran - Guilford CT
Andrew Thurkauf - Danbury CT

Neurogen Corporation - Brandford CT

A61K 31496

51425411, 544376, 544377

Disclosed are compounds of the formula: or the pharmaceutically acceptable acid addition salts thereof wherein: R , R , R , R and R are the same or different and represent hydrogen, halogen, C -C alkyl, C -C alkoxy, C -C alkylthio, hydroxy, amino, mono- or di(C -C )alkylamino, cyano, nitro, trifluoromethyl or trifluoromethoxy; and X is oxygen, a bond, C -C alkylene, or methyleneoxy, which compounds are useful for the treatment and/or prevention of neuropsychological disorders including, but not limited to, schizophrenia, mania, dementia, depression, anxiety, compulsive behavior, substance abuse, Parkinson-like motor disorders and motion disorders related to the use of neuroleptic agents.

6566367, May 20, 2003

Dec 11, 2001

10/013846

Rajagopal Bakthavatchalam - Branford CT
Charles A. Blum - Westbrook CT
Harry L. Brielmann - Guilford CT
James William Darrow - Wallingford CT
Alan Hutchison - Madison CT
Jennifer Tran - Guilford CT
Xiaozhang Zheng - Branford CT
Richard Louis Elliott - East Lyme CT
Marlys Hammond - Salem CT

Pfizer Inc. - New York NY
Neurogen Corporation - Branford CT

C07D47110

514278, 546 17, 546199

Substituted spiro[isobenzofuran-1,4â-piperidin]-3-ones and 3H-spiroisobenzofuran-1,4â-piperidines capable of modulating NPY5 receptor activity are provided. Such compounds may be used to modulate ligand binding to NPY5 receptors in vivo or in vitro, and are particularly useful in the treatment of a variety of disorders (e. g. , eating disorders such as obesity or bulimia, psychiatric disorders, diabetes and cardiovascular disorders such as hypertension) in humans, domesticated companion animals and livestock animals. Pharmaceutical compositions and methods for treating such disorders are provided, as are methods for using such compounds for detecting NPY5 receptors.

6506762, Jan 14, 2003

Sep 29, 2000

09/676941

Raymond F. Horvath - Guilford CT
Jennifer Tran - Guilford CT
Kevin J. Hodgetts - Killingworth CT
Philip A. Carpino - Groton CT
David A. Griffith - Old Saybrook CT

Neurogen Corporation - Branford CT
Pfizer Inc. - New York NY

C07D48704

5142594, 544 80, 544278, 544262, 544276, 544277, 544254, 544281, 544282, 544236, 544256, 544257, 544279, 51425941, 5142632, 51426321, 51426322, 51426323, 5142634, 51426411, 5142651

The present invention also provides a general method to whereby mono-, bi-, or tricyclic heterocycles may be modified to obtain potent antagonists at the NPY receptor. The present invention provides novel, potent, non-peptidic antagonists of NPY receptors, particularly, the NPY receptors, designed from a selection of mono-, bi-, or tri-cyclic heterocyclic cores. This invention relates to novel compounds, compositions, and methods for the treatment of physiological disorders associated with an excess of neuropeptide Y. The novel compounds encompassed by the present invention are those of the formula I-XV. wherein X is N or CR ; W is S, O, or NR ; Y is N or CR ; E, F, and G are each, independently, CR or N; I and J are each, independently, C O, S, O, CR R or NR when single bonded to both adjacent ring atoms, or N, or CR when double bonded to an adjacent ring atom; K is N or CR when double bonded to L or J, or O, S, C O, CR R , or NR when single bonded to both adjacent ring atoms, or N or CR when double bonded to an adjacent ring atom; L is N or CR when single bonded to all atoms to which it is attached, or C (carbon) when double bonded to K; the 6- or 7-membered ring that contains I, J, K, and L may contain from 1 to 3 double bonds, from 0 to 2 heteroatoms, and from 0 to 2 C O groups, wherein the carbon atom of such groups are part of the ring and the oxygen atom is a substituent on the ring; Q is O or NR. Such compounds inhibit the activity of neuropeptide Y at those receptors are useful in treating physiological disorders associated with an excess of neuropeptide Y, including eating disorders, such as, for example, obesity and bulimia, and certain cardiovascular diseases, for example, hypertension.

6544996, Apr 8, 2003

Aug 29, 2001

09/942369

Xiaoyan Zhang - Belle Meade NJ
Jennifer Tran - Guilford CT
He Zhao - Branford CT
Andrew Thurkauf - Danbury CT

Neurogen Corporation - Branford CT

A61K 31495

51425503, 546392, 546394

Disclosed are compounds of the formula: or pharmaceutically acceptable addition salts thereof wherein: R , R , R R and R , R , R , and R represent organic and/or inorganic substituents as defined herein, which compounds are useful for the treatment and/or prevention of neuropsychological disorders including, but not limited to, schizophrenia, mania, dementia, depression, anxiety, compulsive behavior, substance abuse, Parkinson-like motor disorders and motion disorders related to the use of neuroleptic agents.

6696445, Feb 24, 2004

Nov 8, 2002

10/291446

Raymond F. Horvath - Guilford CT
Jennifer N Tran - Guilford CT
Kevin J. Hodgetts - Killingworth CT
Philip A. Carpino - Groton CT
David A. Griffith - Old Saybrook CT

Neurogen Corporation - Branford CT
Pfizer Inc. - New York NY

C07D40112

514245, 544196, 544197, 544198, 544199, 544208, 544209, 544210

The present invention also provides a general method to whereby mono-, bi-, or tricyclic heterocycles may be modified to obtain potent antagonists at the NPY receptor. The present invention provides novel, potent, non-peptidic antagonists of NPY receptors, particularly, the NPY receptors, designed from a selection of mono-, bi-, or tri-cyclic heterocyclic cores. This invention relates to novel compounds, compositions, and methods for the treatment of physiological disorders associated with an excess of neuropeptide Y. The novel compounds encompassed by the present invention are those of the formula I-XV. wherein X is N or CR ; W is S, O, or NR ; Y is N or CR ; E, F, and G are each, independently, CR or N; I and J are each, independently, C O, S, O, CR R or NR when single bonded to both adjacent ring atoms, or N, or CR when double bonded to an adjacent ring atom; K is N or CR when double bonded to L or J, or O, S, C O, CR R , or NR when single bonded to both adjacent ring atoms, or N or CR when double bonded to an adjacent ring atom; L is N or CR when single bonded to all atoms to which it is attached, or C (carbon) when double bonded to K; The 6- or 7-membered ring that contains I, J, K, and L may contain from 1 to 3 double bonds, from 0 to 2 heteroatoms, and from 0 to 2 C O groups, wherein the carbon atom of such groups are part of the ring and the oxygen atom is a substituent on the ring; Q is O or NR. Such compounds inhibit the activity of neuropeptide Y at those receptors are useful in treating physiological disorders associated with an excess of neuropeptide Y, including eating disorders, such as, for example, obesity and bulimia, and certain cardiovascular diseases, for example, hypertension.