David Lee Griffith

US Patent:

6372743, Apr 16, 2002

Filed:

Sep 29, 2000

Appl. No.:

09/676970

Inventors:

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

Assignee:

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

International Classification:

A61K 3153

US Classification:

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

Abstract:

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.

US Patent:

6465651, Oct 15, 2002

Filed:

Aug 3, 2001

Appl. No.:

09/922040

Inventors:

Charles K. Chiu - Guilford CT
David A. Griffith - Old Saybrook CT

Assignee:

Pfizer Inc. - New York NY

International Classification:

C07D48704

US Classification:

544350

Abstract:

This invention relates to a process for preparing compounds of the Formula I, wherein R , R and Pt are as defined in the specification, which are intermediates in the synthesis of certain growth hormone secretagogue compounds. This invention further relates to processes for preparing the growth hormone secretagogues. The invention also relates to the compound of Formula I wherein R is H, R is 2,2,2-trifluoromethyl and Pt is Boc.

US Patent:

6476038, Nov 5, 2002

Filed:

Sep 29, 2000

Appl. No.:

09/676972

Inventors:

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

Assignee:

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

International Classification:

C07D48704

US Classification:

514258, 544281

Abstract:

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.

US Patent:

6506762, Jan 14, 2003

Filed:

Sep 29, 2000

Appl. No.:

09/676941

Inventors:

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

Assignee:

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

International Classification:

C07D48704

US Classification:

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

Abstract:

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.

US Patent:

6603002, Aug 5, 2003

Filed:

Jul 31, 2002

Appl. No.:

10/209834

Inventors:

Charles K. Chiu - Guilford CT
David A. Griffith - Old Saybrook CT

Assignee:

Pfizer Inc. - New York NY

International Classification:

C07D48704

US Classification:

544350

Abstract:

This invention relates to a process for preparing compounds of the Formula I, wherein R , R and Pt are as defined in the specification, which are intermediates in the synthesis of certain growth hormone secretagogue compounds. This invention further relates to processes for preparing the growth hormone secretagogues. The invention also relates to the compound of Formula I wherein R is H, R is 2,2,2-trifluoromethyl and Pt is Boc.

US Patent:

6686471, Feb 3, 2004

Filed:

Jun 5, 2003

Appl. No.:

10/456405

Inventors:

Charles K. Chiu - Guilford CT
David A. Griffith - Old Saybrook CT

Assignee:

Pfizer Inc. - New York NY

International Classification:

C07D48704

US Classification:

544350

Abstract:

This invention relates to a process for preparing compounds of the Formula I, wherein R , R and Pt are as defined in the specification, which are intermediates in the synthesis of certain growth hormone secretagogue compounds. This invention further relates to processes for preparing the growth hormone secretagogues. The invention also relates to the compound of Formula I wherein R is H, R is 2,2,2-trifluoromethyl and Pt is Boc.

US Patent:

6696445, Feb 24, 2004

Filed:

Nov 8, 2002

Appl. No.:

10/291446

Inventors:

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

Assignee:

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

International Classification:

C07D40112

US Classification:

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

Abstract:

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.

US Patent:

7074929, Jul 11, 2006

Filed:

Nov 10, 2003

Appl. No.:

10/705446

Inventors:

Raymond F. Horvath - Guilford CT, US
Jennifer Tran - Guilford CT, US
Stéphane De Lombaert - Madison CT, US
Kevin J. Hodgetts - Killingworth CA, US
Philip A. Carpino - Groton CT, US
David A. Griffith - Old Saybrook CT, US

Assignee:

Neurogen Corp. - Branford CT
Pfizer, Inc. - New York NY

International Classification:

C07D 471/04
A61K 31/4375
A61P 15/10
A61P 3/04

US Classification:

546119, 546117, 546118, 546113, 544276, 544277, 544254, 544281, 544282, 544279, 544262, 544236, 544256, 544 80, 544278, 544257

Abstract:

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 II, IV, V, VII–IX and XI.