Patents by Inventor Hemaka A. Rajapakse

Hemaka A. Rajapakse has filed for patents to protect the following inventions. This listing includes patent applications that are pending as well as patents that have already been granted by the United States Patent and Trademark Office (USPTO).

  • Leucine-rich repeat kinase enzyme activity
    Patent number: 9233977
    Abstract: Disclosed are compounds of Formula (I): and the pharmaceutically acceptable salts thereof, wherein “A” is S—; —SO—, —SO2—, —O— or NRac—, wherein Rac is H, or C1-20 alkyl and R1 through R5 are defined herein. Also disclosed are pharmaceutical formulations comprising a compound of Formula I and methods of treating, managing, or ameliorating diseases amenable to treatment, management, or amelioration by inhibition of LRRK2 kinase activity, for example, Parkinson's disease.
    Type: Grant
    Filed: October 25, 2011
    Date of Patent: January 12, 2016
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: John A. McCauley, Hemaka A. Rajapakse, Thomas J. Greshock, John Sanders, Boyoung Kim, Vanessa L. Rada, Jonathan T. Kern, Heather H. Stevenson, Mark T. Bilodeau
  • LEUCINE-RICH REPEAT KINASE ENZYME ACTIVITY
    Publication number: 20130296317
    Abstract: Disclosed are compounds of Formula (I): and the pharmaceutically acceptable salts thereof, wherein “A” is S—; —SO—, —SO2—, —O— or NRac—, wherein Rac is H, or C1-20 alkyl and R1 through R5 are defined herein. Also disclosed are pharmaceutical formulations comprising a compound of Formula I and methods of treating, managing, or ameliorating diseases amenable to treatment, management, or amelioration by inhibition of LRRK2 kinase activity, for example, Parkinson's disease.
    Type: Application
    Filed: October 25, 2011
    Publication date: November 7, 2013
    Inventors: John A. McCauley, Hemaka A. Rajapakse, Thomas J. Greshock, John Sanders, Boyoung Kim, Vanessa L. Rada, Jonathan T. Kern, Heather H. Stevenson, Mark T. Bilodeau
  • 2-aminoimidazole beta-secretase inhibitors for the treatment of alzheimer's disease
    Patent number: 8492387
    Abstract: The present invention is directed to 2-aminoimidazole compounds of formula (I) which are inhibitors of the beta-secretase enzyme and that are useful in the treatment of diseases in which the beta-secretase enzyme is involved, such as Alzheimer's disease. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the treatment of such diseases in which the beta-secretase enzyme is involved.
    Type: Grant
    Filed: February 18, 2009
    Date of Patent: July 23, 2013
    Assignee: Merck, Sharp & Dohme, Corp.
    Inventors: Ivory D. Hills, Craig A. Coburn, Samuel L. Graham, Keith P. Moore, Philippe G. Nantermet, Hemaka A. Rajapakse, Shawn J. Stachel, Hong Zhu
  • 2,3,4,6-substituted pyridyl derivative compounds useful as beta-secretase inhibitors for the treatment of alzheimer's disease
    Patent number: 8394837
    Abstract: The present invention is directed to 2,3,4,6-substituted pyridyl derivative compounds which are inhibitors of the beta-secretase enzyme and that are useful in the treatment of diseases in which the beta-secretase enzyme is involved, such as Alzheimer's disease. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the treatment of such diseases in which the beta-secretase enzyme is involved.
    Type: Grant
    Filed: November 18, 2005
    Date of Patent: March 12, 2013
    Assignee: Merck, Sharp & Dohme, Corp.
    Inventors: Philippe G. Nantermet, Hemaka A. Rajapakse, Harold G. Selnick, James C. Barrow, Shaun R. Stauffer, Joseph P. Vacca, Keith P. Moore, Shawn J. Stachel, Mattahew G. Stanton
  • Tertiary carbinamines having substituted heterocycles which are active as ?-secretase inhibitors for the treatment of alzheimer's disease
    Patent number: 8338614
    Abstract: The present invention is directed to tertiary carbinamine compounds having substituted heterocycles, which are inhibitors of the beta-secretase enzyme, and are useful in the treatment of diseases in which the beta-secretase enzyme is involved, such as Alzheimer's disease. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the treatment of such diseases in which the beta-secretase enzyme is involved.
    Type: Grant
    Filed: January 13, 2006
    Date of Patent: December 25, 2012
    Assignee: Merck, Sharp & Dohme Corp.
    Inventors: Georgia B. McGaughey, Philippe G. Nantermet, Hemaka A. Rajapakse, Shaun R. Stauffer
  • Spiropiperidine beta-secretase inhibitors for the treatment of alzheimer's disease
    Patent number: 8211904
    Abstract: The present invention is directed to spiropiperidine compounds of formula (I) and tautomers thereof, which are inhibitors of the beta-secretase enzyme and that are useful in the treatment of diseases in which the beta-secretase enzyme is involved, such as Alzheimer's disease. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the treatment of such diseases in which the beta-secretase enzyme is involved.
    Type: Grant
    Filed: July 14, 2006
    Date of Patent: July 3, 2012
    Assignees: Merck, Sharp & Dohme Corp., Sunesis Pharmaceuticals, Inc.
    Inventors: Craig A. Coburn, Melissa S. Egbertson, Samuel L. Graham, Georgia B. McGaughey, Shaun R. Stauffer, Hemaka A. Rajapakse, Philippe G. Nantermet, Shawn J. Stachel, Wenjin Yang, Wanli Lu, Bruce Fahr
  • 2,4,6-substituted pyridyl derivative compounds useful as beta-secretase inhibitors for the treatment of Alzheimer's Disease
    Patent number: 7968571
    Abstract: The present invention is directed to 2,4,6-substituted pyridyl derivative compounds which are inhibitors of the beta-secretase enzyme and that are useful in the treatment of diseases in which the beta-secretase enzyme is involved, such as Alzheimer's disease. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the treatment of such diseases in which the beta-secretase enzyme is involved.
    Type: Grant
    Filed: April 20, 2005
    Date of Patent: June 28, 2011
    Assignee: Merck, Sharp & Dohme, Corp.
    Inventors: James C. Barrow, Georgia B. McGaughey, Philippe G. Nantermet, Hemaka A. Rajapakse, Harold G. Selnick, Shaun R. Stauffer, Joseph P. Vacca, Shawn J. Stachel, Craig A. Coburn, Matthew G. Stanton
  • Macrocyclic aminopyridyl beta-secretase inhibitors for the treatment of Alzheimer's disease
    Patent number: 7951949
    Abstract: The present invention is directed to macrocyclic aminopyridyl compounds represented by general formula (I), which are inhibitors of the beta-secretase enzyme and that are useful in the treatment of diseases in which the beta-secretase enzyme is involved, such as Alzheimer's disease. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the treatment of such diseases in which the beta-secretase enzyme is involved.
    Type: Grant
    Filed: November 18, 2005
    Date of Patent: May 31, 2011
    Assignee: Merck, Sharp & Dohme, Corp.
    Inventors: Philippe G. Nantermet, Hemaka A. Rajapakse, Harold G. Selnick, Keith P. Moore
  • 2-AMINOIMIDAZOLE BETA-SECRETASE INHIBITORS FOR THE TREATMENT OF ALZHEIMER'S DISEASE
    Publication number: 20110034483
    Abstract: The present invention is directed to 2-aminoimidazole compounds of formula (I) which are inhibitors of the beta-secretase enzyme and that are useful in the treatment of diseases in which the beta-secretase enzyme is involved, such as Alzheimer's disease. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the treatment of such diseases in which the beta-secretase enzyme is involved.
    Type: Application
    Filed: February 18, 2009
    Publication date: February 10, 2011
    Inventors: Ivory D. Hills, Craig A. Coburn, Samuel L. Graham, Keith P. Moore, Philippe G. Nantermet, Hemaka A. Rajapakse, Shawn J. Stachel, Hong Zhu
  • 1,3,5-substituted phenyl derivative compounds useful as beta-secretase inhibitors for the treatment of Alzheimer's disease
    Patent number: 7847100
    Abstract: The present invention is directed to 1,3,5-phenyl substituted derivative compounds which are inhibitors of the beta-secretase enzyme and that are useful in the treatment of diseases in which the beta-secretase enzyme is involved, such as Alzheimer's disease. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the treatment of such diseases in which the beta-secretase enzyme is involved.
    Type: Grant
    Filed: April 15, 2005
    Date of Patent: December 7, 2010
    Assignee: Merck, Sharp & Dohme, Inc.
    Inventors: James C. Barrow, Georgia B. McGaughey, Philippe G. Nantermet, Hemaka A. Rajapakse, Harold G. Selnick, Shaun R. Stauffer, Craig A. Coburn
  • Aminomethyl beta-secretase inhibitors for the treatment of alzheimer's disease
    Patent number: 7820674
    Abstract: The present invention is directed to aminomethyl compounds which are inhibitors of the beta-secretase enzyme and that are useful in the treatment of diseases in which the beta-secretase enzyme is involved, such as Alzheimer's disease. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the treatment of such diseases in which the beta-secretase enzyme is involved.
    Type: Grant
    Filed: January 13, 2006
    Date of Patent: October 26, 2010
    Assignee: Merck, Sharp & Dohme Corp.
    Inventors: Craig A. Coburn, Philippe G. Nantermet, Hemaka A. Rajapakse, Harold G. Selnick, Shaun R. Stauffer
  • EPHA4 RTK INHIBITORS FOR TREATMENT OF NEUROLOGICAL AND NEURODEGENERATIVE DISORDERS AND CANCER
    Publication number: 20100113415
    Abstract: The present invention is directed to compounds of generic formula (I) which are inhibitors of ephrin A4. The invention is also directed to pharmaceutical compositions comprising the compounds, and to the use of the compounds and compositions in the treatment of diseases regulated by the EphA4 RTK signaling, such as neurological and neurodegenerative disorders and cancer.
    Type: Application
    Filed: May 28, 2009
    Publication date: May 6, 2010
    Inventors: Hemaka A. Rajapakse, Keith P. Moore, Philippe G. Nantermet, John M. Sanders, Sophie Parmentier-Batteur, Robert J. Mark
  • HIV PROTEASE INHIBITORS
    Publication number: 20100093811
    Abstract: Compounds of Formula I are disclosed: (I), wherein XA, k, R1, R2, R3, R4, R5, R5A, R6, R6A, R7 and R8 are defined herein. The compounds encompassed by Formula I include compounds which are HIV protease inhibitors and other compounds which can be metabolized in vivo to HIV protease inhibitors. The compounds and their pharmaceutically acceptable salts are useful for the prophylaxis or treatment of infection by HIV and the prophylaxis, treatment, or delay in the onset of AIDS. The compounds and their salts can be employed as ingredients in pharmaceutical compositions, optionally in combination with other antivirals, immunomodulators, antibiotics or vaccines.
    Type: Application
    Filed: September 22, 2008
    Publication date: April 15, 2010
    Inventors: Craig A. Coburn, Joseph P. Vacca, Hemaka A. Rajapakse, Kristen L.G. Jones, Philippe Nantermet, James C. Barrow, Keith P. Moore, Steven S. Sharik, Cory Theberge, Abbas M. Walji
  • Macrocyclic tertiary amine beta-secretase inhibitors for the treatment of alzheimer's disease
    Patent number: 7678783
    Abstract: The present invention is directed to macrocyclic tertiary amine compounds represented by general formula (I) which are inhibitors of the beta-secretase enzyme and that are useful in the treatment of diseases in which the beta-secretase enzyme is involved, such as Alzheimer's disease. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the treatment of such diseases in which the beta-secretase enzyme is involved.
    Type: Grant
    Filed: November 14, 2005
    Date of Patent: March 16, 2010
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Philippe G. Nantermet, Hemaka A. Rajapakse, Harold G. Selnick, Stacey Lindsley, Keith P. Moore, Shawn J. Stachel
  • Tricyclic Beta-Secretase Inhibitors for the Treatment of Alzheimer's Disease
    Publication number: 20090182021
    Abstract: The present invention is directed to tricyclic compounds which are inhibitors of the beta-secretase enzyme and that are useful in the treatment of diseases in which the beta-secretase enzyme is involved, such as Alzheimer's disease. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the treatment of such diseases in which the beta-secretase enzyme is involved.
    Type: Application
    Filed: July 28, 2006
    Publication date: July 16, 2009
    Inventors: Philippe G. Nanternet, Hemaka A. Rajapakse
  • Macrocyclic Tertiary Amine Beta-Secretase Inhibitors for the Treatment of Alzheimer's Disease
    Publication number: 20080269302
    Abstract: The present invention is directed to macrocyclic tertiary amine compounds represented by general formula (I) which are inhibitors of the beta-secretase enzyme and that are useful in the treatment of diseases in which the beta-secretase enzyme is involved, such as Alzheimer's disease. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the treatment of such diseases in which the beta-secretase enzyme is involved.
    Type: Application
    Filed: November 14, 2005
    Publication date: October 30, 2008
    Applicant: MERCK & CO., INC.
    Inventors: Philippe G. Nantermet, Hemaka A. Rajapakse, Harold G. Selnick, Stacey Lindsley, Keith P. Moore, Shawn J. Stachel
  • Aminomethyl Beta-Secretase Inhibitors for the Treatment of Alzheimer's Disease
    Publication number: 20080153846
    Abstract: The present invention is directed to aminomethyl compounds which are inhibitors of the beta-secretase enzyme and that are useful in the treatment of diseases in which the beta-secretase enzyme is involved, such as Alzheimer's disease. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the treatment of such diseases in which the beta-secretase enzyme is involved.
    Type: Application
    Filed: January 13, 2006
    Publication date: June 26, 2008
    Inventors: Craig A. Coburn, Philippe G. Nantermet, Hemaka A. Rajapakse, Harold G. Selnick, Shaun R. Stauffer
  • Tertiary Carbinamines Having Substituted Heterocycles Which Are Active As Beta-Secretase Inhibitors For The Treatment Of Alzheimer's Disease
    Publication number: 20080139538
    Abstract: The present invention is directed to tertiary carbinamine compounds having substituted heterocycles, which are inhibitors of the beta-secretase enzyme, and are useful in the treatment of diseases in which the beta-secretase enzyme is involved, such as Alzheimer's disease. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the treatment of such diseases in which the beta-secretase enzyme is involved.
    Type: Application
    Filed: January 13, 2006
    Publication date: June 12, 2008
    Inventors: Georgia B. McGaughey, Philippe G. Nantermet, Hemaka A. Rajapakse, Shaun R. Stauffer
  • Benzylether and benzylamino beta-secretase inhibitors for the treatment of Alzheimer's disease
    Patent number: 7354942
    Abstract: The present invention is directed to benzylether and benzylamino derivative compounds of formula (I) which are inhibitors of the beta-secretase enzyme and that are useful in the treatment of diseases in which the beta-secretase enzyme is involved, such as Alzheimer's disease. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the treatment of such diseases in which the beta-secretase enzyme is involved.
    Type: Grant
    Filed: November 19, 2004
    Date of Patent: April 8, 2008
    Assignee: Merck & Co., Inc.
    Inventors: Philippe G. Nantermet, Hemaka A. Rajapakse, Harold G. Selnick, Shaun R. Stauffer, Mary Beth Young
  • Macrocyclic Aminopyridyl Beta-Secretase Inhibitors For The Treatment Of Alzheimer's Disease
    Publication number: 20080015213
    Abstract: The present invention is directed to macrocyclic aminopyridyl compounds represented by general formula (I), which are inhibitors of the beta-secretase enzyme and that are useful in the treatment of diseases in which the beta-secretase enzyme is involved, such as Alzheimer's disease. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the treatment of such diseases in which the beta-secretase enzyme is involved.
    Type: Application
    Filed: November 18, 2005
    Publication date: January 17, 2008
    Inventors: Philippe Nantermet, Hemaka Rajapakse, Harold Selnick, Keith Moore