Varsha O Gupta

US Patent:

7863266, Jan 4, 2011

Filed:

Jun 6, 2008

Appl. No.:

12/135023

Inventors:

Alan P. Kaplan - San Diego CA, US
Varsha Gupta - San Diego CA, US

Assignee:

Helicon Therapeutics, Inc. - San Diego CA

International Classification:

A61K 31/55
A61K 31/497
A61K 31/455
C07D 243/08
C07D 413/14
C07D 401/14
C07D 471/06

US Classification:

51421704, 5142318, 5142322, 5142328, 51425211, 514315, 514320, 540575, 544126, 544361, 546 82

Abstract:

The invention provides a novel chemical series of formula I, as well as methods of use thereof for binding to the benzodiazepine site of the GABAreceptor and modulating GABA, and use of the compound of formula I for the treatment of GABAreceptor associated disorders. The general structure of formula I is shown below:The invention further provides a method of modulation of one or more GABAsubtypes in an animal comprising administering to the animal an effective amount of a compound of formula (I).

US Patent:

7872002, Jan 18, 2011

Filed:

Jun 6, 2008

Appl. No.:

12/135036

Inventors:

Alan P. Kaplan - San Diego CA, US
Varsha Gupta - San Diego CA, US
Jan W. F. Wasley - Guilford CT, US

Assignee:

Helicon Therapeutics, Inc. - San Diego CA

International Classification:

A61K 31/55
A61K 31/497
A61K 31/445
C07D 243/08
C07D 413/14
C07D 401/14
C07D 471/06

US Classification:

51421704, 5142318, 5142322, 5142328, 51425211, 514315, 514320, 540575, 544126, 544361, 546 82

Abstract:

The invention provides a novel chemical series of formula I, as well as methods of use thereof for binding to the benzodiazepine site of the GABAreceptor and modulating GABA, and use of the compound of formula I for the treatment of GABAreceptor associated disorders. The general structure of formula I is shown below and can exist in tautomeric forms:The invention further provides a method of modulation of one or more GABAsubtypes in an animal comprising administering to the animal an effective amount of a compound of formula (I).

US Patent:

8343957, Jan 1, 2013

Filed:

Nov 29, 2010

Appl. No.:

12/955792

Inventors:

Alan P. Kaplan - San Diego CA, US
Varsha Gupta - Encinitas CA, US

Assignee:

Dart Neuroscience (Cayman) Ltd. - Grand Cayman

International Classification:

A61K 31/55
A61K 31/535
A61K 31/497

US Classification:

514218, 51425201, 51425303, 5142328, 514318, 5142325

Abstract:

The invention provides a novel chemical series of formula I, as well as methods of use thereof for binding to the benzodiazepine site of the GABAreceptor and modulating GABA, and use of the compound of formula I for the treatment of GABAreceptor associated disorders. The general structure of formula I is shown below:The invention further provides a method of modulation of one or more GABAsubtypes in an animal comprising administering to the animal an effective amount of a compound of formula (I).

US Patent:

8497262, Jul 30, 2013

Filed:

Nov 18, 2010

Appl. No.:

12/949619

Inventors:

Alan P. Kaplan - San Diego CA, US
Varsha Gupta - Encinitas CA, US
Jan W. F. Wasley - Guilford CT, US

Assignee:

Dart NeuroScience (Cayman) Ltd - Grand Cayman

International Classification:

A61K 31/55
A61K 31/535
A61K 31/497
A61K 31/445

US Classification:

51421704, 514218, 5142322, 5142328, 51425303, 514315

Abstract:

The invention provides a novel chemical series of formula I, as well as methods of use thereof for binding to the benzodiazepine site of the GABAreceptor and negatively modulating the α5 subtype of GABA, and use of the compound of formula I for the treatment of GABAreceptor associated disorders. The general structure of formula I is shown below:.

US Patent:

8598159, Dec 3, 2013

Filed:

Nov 18, 2010

Appl. No.:

12/949655

Inventors:

Alan P. Kaplan - San Diego CA, US
Varsha Gupta - Encinitas CA, US
Jan W. F. Wasley - Guilford CT, US

Assignee:

Dart Neuroscience (Cayman) Ltd. - Grand Cayman

International Classification:

A61K 31/55
A61K 31/535
A61K 31/445
C07D 243/08
C07D 413/04
C07D 401/04

US Classification:

51421704, 5142322, 5142328, 514315, 540575, 544126, 544361

Abstract:

The invention provides a novel chemical series of formula I, as well as methods of use thereof for binding to the benzodiazepine site of the GABAreceptor and modulating GABA, and use of the compound of formula I for the treatment of GABAreceptor associated disorders. The general structure of formula I is shown below and can exist in tautomeric forms:The invention further provides a method of modulation of one or more GABAsubtypes in an animal comprising administering to the animal an effective amount of a compound of formula (I).

US Patent:

20090005365, Jan 1, 2009

Filed:

Jun 6, 2008

Appl. No.:

12/135045

Inventors:

Alan P. Kaplan - San Diego CA, US
Varsha Gupta - San Diego CA, US
Jan W.F. Wasley - Guilford CT, US

Assignee:

Helicon Therapeutics, Inc. - San Diego CA

International Classification:

A61K 31/496
C07D 401/14
C07D 413/14
A61K 31/5377
A61K 31/551
A61P 25/24
A61P 25/28
A61P 25/18
A61P 25/22
A61K 31/4375
C07D 471/14
C07D 243/08

US Classification:

514218, 544361, 544126, 546 82, 540575, 51425303, 5142328, 514293

Abstract:

The invention provides a novel chemical series of formula I, as well as methods of use thereof for binding to the benzodiazepine site of the GABAreceptor and negatively modulating the α5 subtype of GABA, and use of the compound of formula I for the treatment of GABAreceptor associated disorders. The general structure of formula I is shown below:The invention further provides a method of modulation of one or more GABAsubtypes in an animal comprising administering to the animal an effective amount of a compound of formula (I).

US Patent:

20120095016, Apr 19, 2012

Filed:

Oct 11, 2011

Appl. No.:

13/270982

Inventors:

Varsha Gupta - Encinitas CA, US
Joel Renick - San Diego CA, US
Graeme Freestone - San Diego CA, US
Alan P. Kaplan - San Diego CA, US

Assignee:

Helicon Therapeutics, Inc. - San Diego CA

International Classification:

A61K 31/496
A61K 31/437
A61P 25/22
A61P 25/24
A61P 25/18
A61P 25/28
C07D 471/14
A61P 25/00

US Classification:

51425303, 546 82, 544361, 514293

Abstract:

The invention provides a novel chemical series of formula I, as well as methods of use thereof for binding to the benzodiazepine site of the GABAreceptor and negatively modulating the α5 subtype of GABA, and use of the compound of formula I in the manufacture of a medicament for the treatment of GABAreceptor associated disorders. The invention further provides a method of modulation of one or more GABAsubtypes in an animal comprising administering to the animal an effective amount of a compound of formula (I).

US Patent:

20170312263, Nov 2, 2017

Filed:

May 23, 2017

Appl. No.:

15/603286

Inventors:

- Grand Cayman, KY
Graeme Freestone - San Diego CA, US
Varsha Gupta - Encinitas CA, US
Alan Kaplan - San Diego CA, US
Chi Ching Mak - San Diego CA, US
Benjamin Pratt - Encinitas CA, US
Vincent Santora - San Diego CA, US
Dipanjan Sengupta - San Diego CA, US
Lino Valdez - San Diego CA, US

International Classification:

A61K 31/47
C07D 401/12
C07D 215/60
C07D 215/54
C07D 215/22
C07D 215/20
A61K 31/4709
C07D 471/04
A61K 31/4375

Abstract:

The invention provides a chemical entity of Formula (I)wherein R, R, R, Y, and n have any of the values described herein and compositions comprising such chemical entities; methods of making them; and their use in a wide range of methods, including metabolic and reaction kinetic studies, detection and imaging techniques, and radioactive treatments; and therapies, including inhibiting MAO, and MAO-B selectively, enhancing neuronal plasticity, treating neurological disorders, providing neuroprotection, treating a cognitive impairment associated with a CNS disorder, enhancing the efficiency of cognitive and motor training, providing neurorecovery and neurorehabilitation, enhancing the efficiency of non-human animal training protocols, and treating peripheral disorders (including obesity, diabetes, and cardiometabolic disorders) and their associated co-morbidities.