Ryan Alan Hart

US Patent:

20100234380, Sep 16, 2010

Filed:

May 17, 2007

Appl. No.:

12/301212

Inventors:

Tawfik Gharbaoui - Escondido CA, US
Dipanjan Sengupta - San Diego CA, US
Ashwin M. Krishnan - San Diego CA, US
Nainesh Shah - Escondido CA, US
Ryan M. Hart - San Francisco CA, US
Mark Macias - San Diego CA, US

Assignee:

ARENA PHARMACEUTICALS, INC. - San Diego CA

International Classification:

A61K 31/5377
C07D 413/12
C07D 403/12
C07D 231/12
A61K 31/496
A61K 31/415
A61P 7/00
A61P 25/00
A61P 25/18
A61P 9/00

US Classification:

5142365, 544140, 544371, 5483771, 51425405, 514406

Abstract:

The present invention relates to processes for preparing phenyl-pyrazoles of Formula (I) and salts and pharmaceutical compositions thereof, useful as modulators of 5-HTserotonin receptor activity. The present invention also relates to intermediates used in the processes, and their preparation. The present invention also relates to crystalline forms of 5-HTserotonin receptor modulators, compositions thereof and methods of using the same.

US Patent:

20100240653, Sep 23, 2010

Filed:

Oct 16, 2007

Appl. No.:

12/445795

Inventors:

Vincent J. Santora - Carlsbad CA, US
Ryan M. Hart - San Francisco CA, US
Jason B. Ibarra - La Vegas NV, US
Douglas M. Park - Valley Center CA, US
Albert S. Ren - San Diego CA, US
Graeme Semple - San Diego CA, US
Jeffrey A. Schultz - San Diego CA, US
Brian M. Smith - San Diego CA, US
Jeffrey Smith - San Diego CA, US

International Classification:

A61K 31/4025
A61K 31/5377
A61K 31/506
A61K 31/454
A61K 31/4439
A61K 31/40
C07D 413/12
C07D 403/10
C07D 401/12
C07D 401/10
C07D 409/10
C07D 207/06
A61P 25/28
C07D 405/10
A61P 25/00
A61P 25/24
A61P 3/04
A61P 25/18
A61P 37/08
A61P 11/00

US Classification:

5142355, 514274, 514326, 514343, 514408, 514422, 544141, 544316, 546208, 5462764, 548525, 548578

Abstract:

The present invention relates to certain biphenyl sulfonamide derivatives of Formula (Ia) and pharmaceutical compositions thereof that modulate the activity of the histamine H3-receptor. Compounds of the present invention and pharmaceutical compositions thereof are directed to methods useful in the treatment of histamine H3-associated disorders, such as, cognitive disorders, epilepsy, brain trauma, depression, obesity, disorders of sleep and wakefulness such as narcolepsy, shift-work syndrome, drowsiness as a side effect from a medication, maintenance of vigilance to aid in completion of tasks and the like, cataplexy, hypersomnia, somnolence syndrome, jet lag, sleep apnea and the like, attention deficit hyperactivity disorder (ADHD), schizophrenia, allergies, allergic responses in the upper airway, allergic rhinitis, nasal congestion, dementia, Alzheimer's disease and the like.

US Patent:

20100292288, Nov 18, 2010

Filed:

Jun 6, 2008

Appl. No.:

12/663415

Inventors:

Anthony C. Blackburn - San Diego CA, US
John A. DeMattei - San Diego CA, US
Ryan M. Hart - San Francisco CA, US
Young Mi Khulman - San Diego CA, US
Michael Mesleh - La Jolla CA, US
Jeffrey Smith - San Diego CA, US

Assignee:

ARENA PHARMACEUTICALS, INC. - San Diego CA

International Classification:

A61K 31/40
C07D 207/04
A61P 25/28
A61P 25/08
A61P 25/00
A61P 25/24
A61P 3/04
A61P 25/20
A61P 25/18
A61P 11/00
A61P 29/00

US Classification:

514408, 548578

Abstract:

The present invention is directed to novel salts of (R)-1-{2-[4′-(3-methoxy-propane-1-sulfonyl)-biphenyl-4-yl]-ethyl}-2-methyl-pyrrolidine, and crystalline forms, and compositions thereof that modulate the activity of the histamine H3-receptor and are useful in the treatment of histamine H3-receptor associated disorders, such as, cognitive disorders, epilepsy, brain trauma, depression, obesity, disorders of sleep and wakefulness such as narcolepsy, shift-work syndrome, drowsiness as a side effect from a medication, maintenance of vigilance to aid in completion of tasks and the like, cataplexy, hypersomnia, somnolence syndrome, jet lag, sleep apnea and the like, attention deficit hyperactivity disorder (ADHD), schizophrenia, allergies, allergic responses in the upper airway, allergic rhinitis, nasal congestion, pain, dementia, Alzheimer's disease and the like.

US Patent:

20110207791, Aug 25, 2011

Filed:

Oct 27, 2009

Appl. No.:

13/126564

Inventors:

Lee Alani Selvey - Poway CA, US
Marlon Carlos - Chula Vista CA, US
Paul Maffuid - Carlsbad CA, US
Yun Shan - San Diego CA, US
Ryan M. Hart - San Francisco CA, US
Zezhi Jesse Shao - San Diego CA, US

International Classification:

A61K 31/415
A61P 9/10
A61P 9/00
A61P 9/12
A61P 25/00

US Classification:

514406

Abstract:

The present invention relates to certain compositions of a 5-HTserotonin receptor modulator and methods for their preparation. The compositions disclosed herein are useful for increasing slow wave sleep, improving sleep consolidation, improving sleep maintenance and improving sleep quality, and for treating insomnia and related sleep disorders, dyssomnias, parasomnias and nonrestorative sleep and the like. The compositions disclosed herein are further useful for treating platelet aggregation, coronary artery disease, myocardial infarction, transient ischemic attack, angina, stroke, atrial fibrillation, thrombosis, asthma or symptoms thereof, agitation or symptoms thereof, behavioral disorders, drug induced psychosis, excitative psychosis, Gilles de la Tourette's syndrome, manic disorder, organic or NOS psychosis, psychotic disorders, psychosis, acute schizophrenia, chronic schizophrenia, NOS schizophrenia and related disorders, diabetic-related disorders and progressive multifocal leukoencephalopathy and the like.

US Patent:

20130296321, Nov 7, 2013

Filed:

Jul 3, 2013

Appl. No.:

13/935329

Inventors:

Dipanjan Sengupta - San Diego CA, US
Ashwin M. Krishnan - San Diego CA, US
Nainesh Shah - Rensselaer NY, US
Ryan M. Hart - San Francisco CA, US
Mark Macias - San Diego CA, US
Edward A. Lally - La Jolla CA, US
Jonathan Duffield - San Diego CA, US

International Classification:

C07D 231/12

US Classification:

5142365, 544140

Abstract:

The present invention relates to processes for preparing phenyl-pyrazoles of Formula (I) and salts and pharmaceutical compositions thereof, useful as modulators of 5-HTserotonin receptor activity.The present invention also relates to intermediates used in the processes, and their preparation. The present invention also relates to crystalline forms of 5-HTserotonin receptor modulators, compositions thereof and methods of using the same.

US Patent:

20200397753, Dec 24, 2020

Filed:

Jan 23, 2020

Appl. No.:

16/751029

Inventors:

- San Diego CA, US
Marlon CARLOS - Chula Vista CA, US
Paul MAFFUID - Carlsbad CA, US
Yun SHAN - San Diego CA, US
Ryan M. HART - San Francisco CA, US
Zezhi Jesse SHAO - San Diego CA, US

International Classification:

A61K 31/415
A61K 9/20

Abstract:

The present invention relates to certain compositions of a 5-HTserotonin receptor modulator and methods for their preparation. The compositions disclosed herein are useful for increasing slow wave sleep, improving sleep consolidation, improving sleep maintenance and improving sleep quality, and for treating insomnia and related sleep disorders, dyssomnias, parasomnias and nonrestorative sleep and the like. The compositions disclosed herein are further useful for treating platelet aggregation, coronary artery disease, myocardial infarction, transient ischemic attack, angina, stroke, atrial fibrillation, thrombosis, asthma or symptoms thereof, agitation or symptoms thereof, behavioral disorders, drug induced psychosis, excitative psychosis, Gilles de la Tourette's syndrome, manic disorder, organic or NOS psychosis, psychotic disorders, psychosis, acute schizophrenia, chronic schizophrenia, NOS schizophrenia and related disorders, diabetic-related disorders and progressive multifocal leukoencephalopathy and the like.

US Patent:

20190099402, Apr 4, 2019

Filed:

Sep 27, 2018

Appl. No.:

16/144330

Inventors:

- San Diego CA, US
Marlon CARLOS - Chula Vista CA, US
Paul MAFFUID - Carlsbad CA, US
Yun SHAN - San Diego CA, US
Ryan M. HART - San Francisco CA, US
Zezhi Jesse SHAO - San Diego CA, US

International Classification:

A61K 31/415
A61K 9/20
C07D 231/16
A61K 9/16

Abstract:

The present invention relates to certain compositions of a 5-HTserotonin receptor modulator and methods for their preparation. The compositions disclosed herein are useful for increasing slow wave sleep, improving sleep consolidation, improving sleep maintenance and improving sleep quality, and for treating insomnia and related sleep disorders, dyssomnias, parasomnias and nonrestorative sleep and the like. The compositions disclosed herein are further useful for treating platelet aggregation, coronary artery disease, myocardial infarction, transient ischemic attack, angina, stroke, atrial fibrillation, thrombosis, asthma or symptoms thereof, agitation or symptoms thereof, behavioral disorders, drug induced psychosis, excitative psychosis, Gilles de la Tourette's syndrome, manic disorder, organic or NOS psychosis, psychotic disorders, psychosis, acute schizophrenia, chronic schizophrenia, NOS schizophrenia and related disorders, diabetic-related disorders and progressive multifocal leukoencephalopathy and the like.

US Patent:

20180186748, Jul 5, 2018

Filed:

Sep 11, 2017

Appl. No.:

15/700670

Inventors:

- San Diego CA, US
Dipanjan Sengupta - San Diego CA, US
Ashwin M. Krishnan - San Diego CA, US
Nainesh Shah - Rensselaer NY, US
Ryan M. Hart - San Francisco CA, US
Mark Macias - San Diego CA, US
Edward A. Lally - La Jolla CA, US

International Classification:

C07D 231/12

Abstract:

The present invention relates to processes for preparing phenyl-pyrazoles of Formula (I) and salts and pharmaceutical compositions thereof, useful as modulators of 5-HTserotonin receptor activity.The present invention also relates to intermediates used in the processes, and their preparation. The present invention also relates to crystalline forms of 5-HTserotonin receptor modulators, compositions thereof and methods of using the same.