Alice A Rodriguez

US Patent:

8034806, Oct 11, 2011

Filed:

Oct 31, 2008

Appl. No.:

12/263224

Inventors:

P. Jeffrey Conn - Brentwood TN, US
Craig W. Lindsley - Brentwood TN, US
Charles David Weaver - Franklin TN, US
Alice L. Rodriguez - Nashville TN, US
Colleen M. Niswender - Brentwood TN, US
Carrie K. Jones - Nashville TN, US
Richard Williams - Nashville TN, US

Assignee:

Vanderbilt University - Nashville TN

International Classification:

A01N 43/42
A01N 43/38
A61K 31/47
A61K 31/40
C07D 225/04
C07D 487/00
C07D 491/00
C07D 513/00
C07D 498/00
C07D 471/02
C07D 491/02
C07D 498/02
C07D 513/02
C07D 515/02
C07D 217/22
C07D 487/02
C07D 495/02
C07D 497/02
C07D 209/36

US Classification:

51421208, 514309, 514416, 514418, 540461, 540523, 546113, 546141, 548453, 548484

Abstract:

In one aspect, the invention relates to bicyclic MGluR5 positive allosteric modulators, for example 6-(phenylethynyl)-3,4-dihydroisoquinolin-1(2H)-one, derivatives thereof, and related compounds, which are useful as positive allosteric modulators of the metabotropic glutamate receptor subtype 5 (mGluR5); synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating neurological and psychiatric disorders associated with glutamate dysfunction using the compounds and compositions. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.

US Patent:

8501757, Aug 6, 2013

Filed:

Sep 17, 2010

Appl. No.:

12/885420

Inventors:

P. Jeffrey Conn - Brentwood TN, US
Craig W. Lindsley - Brentwood TN, US
Kyle A. Emmitte - Spring Hill TN, US
Charles David Weaver - Franklin TN, US
Alice L. Rodriguez - Nashville TN, US
Andrew S. Felts - Nashville TN, US
Carrie K. Jones - Nashville TN, US
Brittney S. Bates - Nashville TN, US
Brian A. Chauder - Smyrna TN, US

Assignee:

Vanderbilt University - Nashville TN

International Classification:

A61K 31/505
A61K 31/44
C07D 239/02
C07D 403/12
C07D 401/12
C07D 213/62
A61K 31/4965

US Classification:

514272, 51425505, 514333, 514335

Abstract:

Disclosed are negative allosteric modulators of the metabotropic glutamate receptor subtype 5 (mGluR5); synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating neurological and psychiatric disorders associated with glutamate dysfunction using the compounds and compositions. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.

US Patent:

8569308, Oct 29, 2013

Filed:

Sep 17, 2010

Appl. No.:

12/885245

Inventors:

P. Jeffrey Conn - Brentwood TN, US
Craig W. Lindsley - Brentwood TN, US
Kyle A. Emmitte - Spring Hill TN, US
Charles David Weaver - Franklin TN, US
Alice L. Rodriguez - Nashville TN, US
Andrew S. Felts - Nashville TN, US
Carrie K. Jones - Nashville TN, US
Brittney S. Bates - Nashville TN, US

Assignee:

Vanderbilt University - Nashville TN

International Classification:

A01N 37/30
A61K 31/205

US Classification:

51425505, 544295

Abstract:

Disclosed are negative allosteric modulators of the metabotropic glutamate receptor subtype 5 (mGluR5); synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating neurological and psychiatric disorders associated with glutamate dysfunction using the compounds and compositions. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.

US Patent:

8598345, Dec 3, 2013

Filed:

Sep 17, 2010

Appl. No.:

12/885289

Inventors:

P. Jeffrey Conn - Brentwood TN, US
Craig W. Lindsley - Brentwood TN, US
Kyle A. Emmitte - Spring Hill TN, US
Charles David Weaver - Franklin TN, US
Alice L. Rodriguez - Nashville TN, US
Andrew S. Felts - Nashville TN, US
Carrie K. Jones - Nashville TN, US
Brittney S. Bates - Nashville TN, US

Assignee:

Vanderbilt University - Nashville TN

International Classification:

C07D 401/12
C07D 213/65
A61P 29/00
A61P 25/22

US Classification:

544333, 546261

Abstract:

Disclosed are negative allosteric modulators of the metabotropic glutamate receptor subtype 5 (mGluR5); synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating neurological and psychiatric disorders associated with glutamate dysfunction using the compounds and compositions. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.

US Patent:

20070208028, Sep 6, 2007

Filed:

Sep 20, 2006

Appl. No.:

11/523873

Inventors:

P. Conn - Brentwood TN, US
Alice Rodriguez - Nashville TN, US
Carrie Jones - Nashville TN, US

International Classification:

A61K 31/506
A61K 31/497
A61K 31/4965
A61K 31/44

US Classification:

514252100, 514277000, 514256000

Abstract:

Provided is a method of treating conditions and disorders for which full mGluR5 antagonists are potentially effective, such as, e.g., anxiety, epilepsy, schizophrenia and other psychotic disorders, Parkinson's disease, addictive disorders, and the like in a subject in need of such treatment, comprising administration to such subject of a therapeutically effective amount of a partial, non-competitive mGluR5 antagonist compound of the invention. Specific examples of partial MgluR5 antagonists provided include those compounds having the formula: wherein: Z is, independently N or —CH—, provided that one, and only one Z is N; R is halogen (e.g., Br, F and the like), alkyl (e.g., methyl), alkenyl (e.g., CH═CH2, aryl (e.g., phenyl), heterocyclic (e.g., thiophenyl).

US Patent:

20090042855, Feb 12, 2009

Filed:

Jun 3, 2008

Appl. No.:

12/132289

Inventors:

P. Jeffrey Conn - Brentwood TN, US
Craig W. Lindsley - Brentwood TN, US
Charles David Weaver - Franklin TN, US
Alice L. Rodriguez - Nashville TN, US
Colleen M. Niswender - Brentwood TN, US
Carrie K. Jones - Nashville TN, US
Richard Williams - Nashville TN, US

International Classification:

A61K 31/445
A61P 25/00
C07D 211/60
C07D 295/14
C07D 401/04
A61K 31/45
A61K 31/4965
A61K 31/496
A61K 31/5377
A61K 31/5375
A61K 31/397

US Classification:

51421018, 546226, 546221, 544176, 544365, 544391, 544360, 51421017, 5142372, 5142378, 5142375, 51425313, 514327, 514330, 51425501

Abstract:

In one aspect, the invention relates to compounds, including phenylethynylbenzamide derivatives, cycloalkylethynylbenzamide derivatives, styrylbenzamide derivatives, 4-(3-phenyl-1,2,4-oxadiazol-5-yl)benzamide derivatives, 4-(pyridinylethynyl)benzamide derivatives, and N-phenylterephthalamide derivatives, which are useful as positive allosteric modulators of the metabotropic glutamate receptor subtype 5 (mGluR5); synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating neurological and psychiatric disorders associated with glutamate dysfunction using the compounds and compositions. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.

US Patent:

20110152299, Jun 23, 2011

Filed:

Sep 17, 2010

Appl. No.:

12/885378

Inventors:

P. Jeffrey Conn - Brentwood TN, US
Craig W. Lindsley - Brentwood TN, US
Kyle A. Emmitte - Spring Hill TN, US
Charles David Weaver - Franklin TN, US
Alice L. Rodriguez - Nashville TN, US
Andrew S. Felts - Nashville TN, US
Carrie K. Jones - Nashville TN, US

International Classification:

A61K 31/506
C07D 401/12
A61K 31/4439
C07D 403/12
A61P 25/22
A61P 25/16
A61P 29/00
A61P 1/04

US Classification:

514269, 5462707, 514342, 544298

Abstract:

Disclosed are negative allosteric modulators of the metabotropic glutamate receptor subtype 5 (mGluR5); synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating neurological and psychiatric disorders associated with glutamate dysfunction using the compounds and compositions. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention

US Patent:

20120028955, Feb 2, 2012

Filed:

Oct 10, 2011

Appl. No.:

13/269933

Inventors:

P. Jeffrey Conn - Brentwood TN, US
Craig W. Lindsley - Brentwood TN, US
Charles David Weaver - Franklin TN, US
Alice L. Rodriguez - Nashville TN, US
Colleen M. Niswender - Brentwood TN, US
Carrie K. Jones - Nashville TN, US
Richard Williams - Nashville TN, US

International Classification:

A61K 31/472
C07D 413/06
C07D 209/48
C07D 209/46
C07D 401/06
A61K 31/4725
A61K 31/5377
A61K 31/4035
A61K 31/496
A61P 25/28
A61P 25/00
A61P 25/18
A61P 25/30
A61P 25/14
A61P 25/08
A61P 25/06
A61P 3/10
A61P 3/04
A61P 25/24
C07D 217/24

US Classification:

51421021, 546141, 544128, 548480, 548472, 544363, 514309, 5142352, 514417, 514416, 51425305

Abstract:

In one aspect, the invention relates to bicyclic mGluR5 positive allosteric modulators, for example 6-(phenylethynyl)-3,4-dihydroisoquinolin-1(2H)-one, derivatives thereof, and related compounds, which are useful as positive allosteric modulators of the metabotropic glutamate receptor subtype 5 (mGluR5); synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating neurological and psychiatric disorders associated with glutamate dysfunction using the compounds and compositions. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.