Katsumasa N Nakajima

US Patent:

8084448, Dec 27, 2011

Filed:

Mar 29, 2007

Appl. No.:

12/295545

Inventors:

Alan Neubert - North Attleborough MA, US
David Barnes - Waban MA, US
Young-Shin Kwak - Lexington MA, US
Katsumasa Nakajima - Winchester MA, US
Gregory Raymond Bebernitz - Stow MA, US
Gary Mark Coppola - Budd Lake NJ, US
Louise Kirman - Swampscott MA, US
Michael H. Serrano-Wu - Belmont MA, US
Travis Stams - Stow MA, US
Sidney Wolf Topiol - Fair Lawn NJ, US
Thalaththani Ralalage Vedananda - Shrewsbury MA, US
James Richard Wareing - Stow MA, US

Assignee:

Novartis AG - Basel

International Classification:

A61K 31/55
A61K 31/445
A61K 31/41
C07D 487/00
C07D 401/00
C07D 285/10

US Classification:

51421207, 514326, 514362, 540523, 546209, 548135

Abstract:

Compounds of the formula.

US Patent:

20080262050, Oct 23, 2008

Filed:

Dec 6, 2006

Appl. No.:

12/096439

Inventors:

David Barnes - Waban MA, US
Gregory Raymond Bebernitz - Stow MA, US
Gary Mark Coppola - Budd Lake NJ, US
Katsumasa Nakajima - Winchester MA, US
Travis Stams - Stow MA, US
Sidney Wolf Topiol - Fair Lawn NJ, US
Thalaththani Ralalage Vedananda - Shrewsbury MA, US
James Richard Wareing - Stow MA, US

International Classification:

A61K 31/433
C07D 285/10
A61P 3/00
A61P 25/00
A61P 9/00
C07D 417/02

US Classification:

514362, 548135

Abstract:

Compounds of the formulaare inhibitors of protein tyrosine phosphatases (PTPases) and, thus, may be employed for the treatment of conditions mediated by PTPase activity. The compounds of the present invention may also be employed as inhibitors of other enzymes characterized with a phosphotyrosine binding region such as the SH2 domain. The compounds of formula (I) may be employed for prevention and/or treatment of insulin resistance associated with obesity, glucose intolerance, diabetes mellitus, hypertension and ischemic diseases of the large and small blood vessels, conditions that accompany type-2 diabetes, including hyperlipidemia, hypertriglyceridemia, atherosclerosis, vascular restenosis, irritable bowel syndrome, pancreatitis, adipose cell tumors and carcinomas such as liposarcoma, dyslipidemia, and other disorders where insulin resistance is indicated. In addition, the compounds of the present invention may be employed to treat and/or prevent cancer, osteoporosis, neurodegenerative and infectious diseases, and diseases involving inflammation and the immune system.

US Patent:

20080293782, Nov 27, 2008

Filed:

Dec 6, 2006

Appl. No.:

12/096421

Inventors:

David Barnes - Waban MA, US
Gary Mark Coppola - Budd Lake NJ, US
Robert Edson Damon - Hopkinton MA, US
Katsumasa Nakajima - Winchester MA, US
Brian Christopher Raudenbush - Beacon Falls CT, US
Travis Stams - Stow MA, US
Sidney Wolf Topiol - Fair Lawn NJ, US
Thalaththani Ralalage Vedananda - Shrewsbury MA, US

International Classification:

A61K 31/433
C07D 285/10
A61P 3/10
A61P 3/04
A61P 9/10
A61P 25/28
A61P 35/00

US Classification:

514362, 548135

Abstract:

Compounds of the formulaare inhibitors of protein tyrosine phosphatases (PTPases) and, thus, may be employed for the treatment of conditions mediated by PTPase activity. The compounds of the present invention may also be employed as inhibitors of other enzymes characterized with a phosphotyrosine binding region such as the SH2 domain. Accordingly, the compounds of formula (I) may be employed for prevention and/or treatment of insulin resistance associated with obesity, glucose intolerance, diabetes mellitus, hypertension and ischemic diseases of the large and small blood vessels, conditions that accompany type-2 diabetes, including hyperlipidemia, hypertriglyceridemia, atherosclerosis, vascular restenosis, irritable bowel syndrome, pancreatitis, adipose cell tumors and carcinomas such as liposarcoma, dyslipidemia, and other disorders where insulin resistance is indicated. In addition, the compounds of the present invention may be employed to treat and/or prevent cancer, osteoporosis, neurodegenerative and infectious diseases, and diseases involving inflammation and the immune system.

US Patent:

20100022513, Jan 28, 2010

Filed:

Jul 14, 2009

Appl. No.:

12/502669

Inventors:

Cornelia Jutta Forster - Cambridge MA, US
Young-Shin Kwak - Cambridge MA, US
Katsumasa Nakajima - Cambridge MA, US
Bing Wang - Cambridge MA, US

International Classification:

A61K 31/553
C07D 249/14
C07D 281/06
C07D 413/12
A61K 31/4196
A61K 31/5377
A61P 3/10
A61P 3/04

US Classification:

51421115, 5482654, 540544, 544132, 514383, 5142362

Abstract:

The invention relates to compounds of formula (I):where A is an optionally substituted heteroaryl, useful for treating disorders mediated by acyl coA-diacylglycerol acyl transferase 1 (DGAT1), e.g. metabolic disorders. The invention also provides methods of treating such disorders, and compounds and compositions etc. for their treatment.

US Patent:

20220315582, Oct 6, 2022

Filed:

Jul 31, 2020

Appl. No.:

16/973836

Inventors:

- Basel, CH
Tracy CHEN - Litchfield NH, US
Jian DING - Bedford MA, US
Christy FRYER - Cambridge MA, US
Yuko ISOME - Arlington MA, US
Marie-Helene LARRAUFIE - Barcelona, ES
Katsumasa NAKAJIMA - Winchester MA, US
Nik SAVAGE - Somerville MA, US
Ariel Sterling TWOMEY - Everett MA, US

International Classification:

C07D 471/10
A61P 35/00

Abstract:

The present invention relates to novel tricyclic compounds that are AKR1C3 dependent KARS inhibitor, processes for their preparation, pharmaceutical compositions, and medicaments containing them, and their use in diseases and disorders mediated by an AKR1C3 dependent KARS inhibitor.

US Patent:

20230091510, Mar 23, 2023

Filed:

May 19, 2020

Appl. No.:

17/612280

Inventors:

- Basel, CH
Katsumasa NAKAJIMA - Winchester MA, US
Matthew T. BURGER - Belmont MA, US
Joseph Anthony D'ALESSIO - Boston MA, US
Eric MCNEILL - Arlington MA, US
Mark G, PALMERO - Ridge NH, US
Bing YU - Belmont MA, US
Qiang ZHANG - East Brunswick NJ, US

International Classification:

A61K 47/68
A61K 47/54
A61K 47/60
A61K 47/61
A61P 35/00
C07K 16/28
C07K 5/062

Abstract:

Provided herein are linkers, linker-drug groups and anti-body-drug conjugates comprising hydrophilic groups.

US Patent:

20230092679, Mar 23, 2023

Filed:

May 19, 2020

Appl. No.:

17/613006

Inventors:

- Basel, CH
- Suresnes Cedex, FR
Frédéric Colland - Puiseux-en-France, FR
Marton Csekei - Dunakeszi, HU
Lea Delacour - Luxembourg, LU
Patrice Desos - Bois Colombes, FR
Olivier Geneste - Rueil-Malmaison, FR
Jean-Michel Henlin - Suresnes, FR
Vesela Kostova - Saint Cloud, FR
Andras Kotschy - Torokbalint, HU
Ana Leticia Maragno - Croissy-sur-Seine, FR
Eric McNeill - Arlington MA, US
Mark G. Palermo - Ringe NH, US
Francesca Rocchetti - Paris, FR
Jérôme Starck - Rueill-Malmaison, FR
Bing Yu - Belmont MA, US
Qiang Zhang - East Brunswick NJ, US
Ágnes Proszenyák - Budapest, HU
Szabolcs Sipos - Budapest, HU
Zhuoliang Chen - Belmont MA, US
Katsumasa Nakajima - Winchester MA, US
Joseph Anthony D'Alessio - Boston MA, US

International Classification:

A61K 47/68
A61K 47/65
A61K 31/505
A61P 35/00

Abstract:

Antibody-drug conjugates that bind to human oncology targets are disclosed. The antibody-drug conjugates comprise an Mcl-1 inhibitor drug moiety. The disclosure further relates to methods and compositions for use in the treatment of cancers by administering the antibody-drug conjugates provided herein. Linker-drug conjugates comprising an Mcl-1 inhibitor drug moiety and methods of making same are also disclosed.

US Patent:

20230081720, Mar 16, 2023

Filed:

May 19, 2020

Appl. No.:

17/613020

Inventors:

- Basel, CH
- Suresnes Cedex, FR
Frédéric Colland - Puiseux-en-France, FR
Marton Csekei - Dunakeszi, HU
Lea Delacour - Luxembourg, LU
Patrice Desos - Bois Colombes, FR
Olivier Geneste - Rueil-Malmaison, FR
Jean-Michel Henlin - Suresnes, FR
Vesela Kostova - Saint Cloud, FR
Andras Kotschy - Torokbalint, HU
Ana Leticia Maragno - Croissy-sur-Seine, FR
Eric McNeill - Arlington MA, US
Mark G. Palermo - Ringe NH, US
Francesca Rocchetti - Paris, FR
Jérôme Starck - Rueill-Malmaison, FR
Bing Yu - Belmont MA, US
Qiang Zhang - East Brunswick NJ, US
Ágnes Proszenyák - Budapest, HU
Szabolcs Sipos - Budapest, HU
Zhuoliang Chen - Belmont MA, US
Katsumasa Nakajima - Winchester MA, US
Joseph Anthony D'Alessio - Boston MA, US
John William Blankenship - Acton MA, US

International Classification:

A61K 47/68

Abstract:

Anti-CD74 antibody-drug conjugates are disclosed. The anti-CD74 antibody-drug conjugates comprise an Mcl-1 inhibitor drug moiety and an anti-CD74 antibody or antigen-binding fragment thereof that binds an antigen target, e.g., an antigen expressed on a tumor or other cancer cell. The disclosure further relates to methods and compositions for use in the treatment of cancers by administering the antibody-drug conjugates provided herein. Linker-drug conjugates comprising an Mcl-1 inhibitor drug moiety and methods of making same are also disclosed.