Anna Aldona Zabierek, Age 4485 Heritage Dr, Tewksbury, MA 01876

7834026, Nov 16, 2010

Nov 17, 2006

12/085396

Scott C. Berk - Cambridge MA, US
Joshua Close - Franklin MA, US
Christopher Hamblett - Boston MA, US
Richard W. Heidebrecht - Brookline MA, US
Solomon D. Kattar - Medford MA, US
Laura T. Kliman - Cambridge MA, US
Dawn M. Mampreian - Brookline MA, US
Joey L. Methot - Westwood MA, US
Thomas Miller - Brookline MA, US
David L. Sloman - Boston MA, US
Matthew G. Stanton - Medfield MA, US
Paul Tempest - Brookline MA, US
Anna A. Zabierek - East Kingston NH, US

Merck Sharp & Dohme Corp. - Rahway NJ

A01N 43/42
A01N 43/12
A01N 43/26
A61K 31/44
A61K 31/34
A61K 31/335
C07D 237/00
C07D 239/00
C07D 241/00
C07D 491/10
C07D 491/20
C07D 495/10
C07D 495/20
C07D 497/10
C07D 497/20
C07D 311/96
C07D 313/06
C07D 313/20
C07D 315/00

514278, 514462, 544230, 546 19, 549331

The present invention relates to a novel class of substituted spirocyclic compounds, represented by the following structural Formula: I Wherein A, B and D are independently selected from CR, NR, C(O) and O; E is selected from a bond, CR, NR, C(O) and O; wherein at least one of A, B, D or E is CR; and provided that when A is O, then E is not O; G is CR; R is selected from NHand OH; These compounds can inhibit histone deacetylase and are suitable for use in selectively inducing termin differentiation, and arresting cell growth and/or apoptosis of neoplastic cells, thereby inhibiting proliferation of such cells. Thus, the compounds of the present invention are useful in treating a patient having a tumor characterized by proliferation of neoplastic cells. The compounds of the invention may also be useful in the prevention and treatment of TRX-mediated diseases, such as autoimmune, allergic and inflammatory diseases, and in the prevention and/or treatment of diseases of the central nervous system (CNS), such as neurodegenerative diseases. The present invention further provides pharmaceutical compositions comprising the compounds of the instant invention and safe dosing regimens of these pharmaceutical compositions, which are easy to follow, and which result in a therapeutically effective amount of these compounds in vivo.

8278335, Oct 2, 2012

Apr 9, 2009

12/988705

Michelle R. Machacek - Brookline MA, US
Andrew Haidle - Cambridge MA, US
Anna A. Zabierek - Boston MA, US
Kaleen M. Konrad - Boston MA, US
Michael D. Altman - Needham MA, US

Merck Sharp & Dohme Corp. - Rahway NJ

A01N 43/40
A61K 31/44

514342, 51425205, 5462697, 544238

The instant invention provides for compounds that inhibit the four known mammalian JAK kinases (JAK1, JAK2, JAK3 and TYK2) and PDK1. The invention also provides for compositions comprising such inhibitory compounds and methods of inhibiting the activity of JAK1, JAK2, JAK3, TYK2 and PDK1 by administering the compound to a patient in need of treatment for myeloproliferative disorders or cancer.

8349825, Jan 8, 2013

Oct 26, 2010

12/912094

Dawn M. Mampreian - Brookline MA, US
Joey L. Methot - Westwood MA, US
Thomas Miller - Brookline MA, US
Paul Tempest - Brookline MA, US
Anna A. Zabierek - East Kingston NH, US

Merck Sharp & Dohme Corp. - Rahway NJ

A61K 31/00
A61K 31/445
C07D 221/00
C07D 205/00

51421021, 514317, 514326, 546 15, 548950

The present invention relates to a novel class of substituted spirocyclic compounds. These compounds can inhibit histone deacetylase and are suitable for use in selectively inducing terminal differentiation, and arresting cell growth and/or apoptosis of neoplastic cells, thereby inhibiting proliferation of such cells. Thus, the compounds of the present invention are useful in treating a patient having a tumor characterized by proliferation of neoplastic cells. The compounds of the invention may also be useful in the prevention and treatment of TRX-mediated diseases, such as autoimmune, allergic and inflammatory diseases, and in the prevention and/or treatment of diseases of the central nervous system (CNS), such as neurodegenerative diseases. The present invention further provides pharmaceutical compositions comprising the compounds of the instant invention and safe dosing regimens of these pharmaceutical compositions, which are easy to follow, and which result in a therapeutically effective amount of these compounds in vivo.

8367706, Feb 5, 2013

Jun 16, 2008

12/665045

Michael Altman - Cambridge MA, US
Matthew Christopher - Wallingford CT, US
Jonathan B. Grimm - Newton MA, US
Andrew Haidle - Cambridge MA, US
Kaleen Konrad - Newton MA, US
Jongwon Lim - Lexington MA, US
Rachel N. MacCoss - Brookline MA, US
Michelle Machacek - Brookline MA, US
Ekundayo Osimboni - Ashland MA, US
Ryan D. Otte - Natick MA, US
Tony Siu - Brookline MA, US
Kerrie Spencer - Woonsocket RI, US
Brandon Taoka - Allston MA, US
Paul Tempest - Brookline MA, US
Kevin Wilson - West Newton MA, US
Hyun Chong Woo - Brookline MA, US
Jonathan Young - Southborough MA, US
Anna Zabierek - Salem MA, US

Merck Sharp & Dohme Corp. - Rahway NJ

A61K 31/4436
C07D 409/12

514336, 5462814

The instant invention provides for compounds that inhibit the four known mammalian JAK kinases (JAK1, JAK2, JAK3 and TYK2) and PDK1. The invention also provides for compositions comprising such inhibitory compounds and methods of inhibiting the activity of JAK1, JAK2, JAK3 TYK2 and PDK1 by administering the compound to a patient in need of treatment for myeloproliferative disorders or cancer.

2007011, May 24, 2007

Nov 16, 2006

11/600426

Scott Berk - Cambridge MA, US
Joshua Close - Franklin MA, US
Christopher Hamblett - Boston MA, US
Richard Heidebrecht - Brookline MA, US
Solomon Kattar - Medford MA, US
Laura Kliman - Cambridge MA, US
Dawn Mampreian - Brookline MA, US
Joey Methot - Westwood MA, US
Thomas Miller - Brookline MA, US
David Sloman - Boston MA, US
Matthew Stanton - Medfield MA, US
Paul Tempest - Brookline MA, US
Anna Zabierek - East Kingston NH, US

A61K 31/4747
C07D 471/10

514278000, 546015000

The present invention relates to a novel class of substituted spirocyclic compounds. These compounds can inhibit histone deacetylase and are suitable for use in selectively inducing terminal differentiation, and arresting cell growth and/or apoptosis of neoplastic cells, thereby inhibiting proliferation of such cells. Thus, the compounds of the present invention are useful in treating a patient having a tumor characterized by proliferation of neoplastic cells. The compounds of the invention may also be useful in the prevention and treatment of TRX-mediated diseases, such as autoimmune, allergic and inflammatory diseases, and in the prevention and/or treatment of diseases of the central nervous system (CNS), such as neurodegenerative diseases. The present invention further provides pharmaceutical compositions comprising the compounds of the instant invention and safe dosing regimens of these pharmaceutical compositions, which are easy to follow, and which result in a therapeutically effective amount of these compounds in vivo.

2010021, Aug 26, 2010

Sep 30, 2008

12/681634

Solomon Kattar - Arlington MA, US
Thomas A. Miller - Brookline MA, US
Karin M. Otte - Natick MA, US
Phieng Siliphaivanh - Newton MA, US
Laura Surdi - Natick MA, US
Paul Tempest - Brookline MA, US
Anna A. Zabierek - Salem MA, US

A61K 31/166
C07C 233/64
C07D 319/16
C07D 265/30
A61K 31/357
A61K 31/5375
A61P 35/00

5142378, 564156, 549362, 544169, 514616, 514452

The present invention relates to a novel class of N-hydroxy-naphthalene dicarboxamide and N-hydroxy-biphenyl-dicarboxamide derivatives. The N-hydroxy-naphthalene dicarboxamide and N-hydroxy-biphenyl-dicarboxamide compounds can be used to treat cancer. The N-hydroxy-naphthalene dicarboxamide and N-hydroxy-biphenyl-dicarboxamide compounds can also inhibit histone deacetylase and are suitable for use in selectively inducing terminal differentiation, and arresting cell growth and/or apoptosis of neoplastic cells, thereby inhibiting proliferation of such cells. Thus, the compounds of the present invention are useful in treating a patient having a tumor characterized by proliferation of neoplastic cells. The compounds of the invention may also be useful in the prevention and treatment of TRX-mediated diseases, such as autoimmune, allergic and inflammatory diseases, and in the prevention and/or treatment of diseases of the central nervous system (CNS), such as neurodegenerative diseases. The present invention further provides pharmaceutical compositions comprising the N-hydroxy-naphthalene dicarboxamide and N-hydroxy-biphenyl-dicarboxamide derivatives and safe dosing regimens of these pharmaceutical compositions, which are easy to follow, and which result in a therapeutically effective amount of the N-hydroxy-naphthalene dicarboxamide and N-hydroxy-biphenyl-dicarboxamide derivatives in vivo.

2013013, May 23, 2013

Dec 19, 2012

13/719999

Joshua Close - Franklin MA, US
Christopher Hamblett - West Roxbury MA, US
Richard W. Heidebrecht - Brookline MA, US
Solomon D. Kattar - Arlington MA, US
Laura T. Kliman - Brighton MA, US
Dawn M. Mampreian Hoffman - Boston MA, US
Joey L. Methot - Westwood MA, US
Thomas Miller - Brookline MA, US
David L. Soloman - Boston MA, US
Matthew G. Stanton - Marlton NJ, US
Paul Tempest - Brookline MA, US
Anna Z. Zabierek - Watertown MA, US

Merck Sharp & Dohme Corp. - Rahway NJ

C07D 471/10
C07D 498/10
C07D 491/107
C07D 487/10

51421018, 546 20, 514278, 546 15, 546 16, 544230, 514275, 5142102

The present invention relates to a novel class of substituted spirocyclic compounds. These compounds can inhibit histone deacetylase and are suitable for use in selectively inducing terminal differentiation, and arresting cell growth and/or apoptosis of neoplastic cells, thereby inhibiting proliferation of such cells. Thus, the compounds of the present invention are useful in treating a patient having a tumor characterized by proliferation of neoplastic cells. The compounds of the invention may also be useful in the prevention and treatment of TRX-mediated diseases, such as autoimmune, allergic and inflammatory diseases, and in the prevention and/or treatment of diseases of the central nervous system (CNS), such as neurodegenerative diseases. The present invention further provides pharmaceutical compositions comprising the compounds of the instant invention and safe dosing regimens of these pharmaceutical compositions, which are easy to follow, and which result in a therapeutically effective amount of these compounds in vivo.

2015017, Jun 25, 2015

Jun 18, 2013

14/409147

- Rahway NJ, US
- Kirkland, CA
John Michael Ellis - Needham MA, US
Kaleen Konrad Childers - Medfield MA, US
Anthony Donofrio - Cambridge MA, US
Michael D. Altman - Needham MA, US
Andrew M. Haidle - Cambridge MA, US
Anna Zabierek - Watertown MA, US
Matthew Christopher - Brookline MA, US
Jonathan Grimm - Ashburn VA, US
Jason Burch - Redwood City CA, US
Maria Emilia Di Francesco - Houston TX, US
Alessia Petrocchi - Houston TX, US
Christian Beaulieu - Laval, CA
Vouy Linh Truong - Pierrefonds, CA
Alan B. Northrup - Reading MA, US
Marc Blouin - Saint-Lazare, CA

C07D 403/12
C07D 401/14

The present invention provides novel imidazole analogs of Formula I which are potent inhibitors of spleen tyrosine kinase, and are useful in the treatment and prevention of diseases mediated by said enzyme, such as asthma, COPD, rheumatoid arthritis, and cancer.