公开(公告)号：US10821100B2

公开(公告)日：2020-11-03

申请号：US16423992

申请日：2019-05-28

Applicant: Glenmark Pharmaceuticals S.A.

Inventor： Laxmikant A. Gharat ,  Nagarajan Muthukaman ,  Neelima Khairatkar-Joshi ,  Vidya G. Kattige

IPC: A61K31/4196 ,  C07D401/04 ,  C07D401/10 ,  C07D403/04 ,  C07D403/10 ,  C07D403/12 ,  C07D405/12 ,  C07D409/14 ,  C07D413/10 ,  C07D417/10 ,  C07D417/12 ,  A61K31/4245 ,  A61K31/428 ,  A61K31/433 ,  A61K31/4439 ,  A61K31/5377 ,  C07D249/12 ,  C07D413/12 ,  A61K31/422

Abstract: The present disclosure is directed to compounds of formula (I), and pharmaceutically acceptable salts thereof, as mPGES-1 inhibitors. These compounds are inhibitors of the microsomal prostaglandin E synthase-1 (mPGES-1) enzyme and are therefore useful in the treatment of pain and/or inflammation from a variety of diseases or conditions, such as asthma, osteoarthritis, rheumatoid arthritis, acute or chronic pain and neurodegenerative diseases.

公开(公告)号：US20180200229A1

公开(公告)日：2018-07-19

申请号：US15919460

申请日：2018-03-13

Applicant: Glenmark Pharmaceuticals S.A.

Inventor： Laxmikant A. Gharat ,  Nagarajan Muthukaman ,  Neelima Khairatkar-Joshi ,  Vidya G. Kattige

IPC: A61K31/4196 ,  A61K31/4245 ,  C07D401/10 ,  C07D413/12 ,  A61K31/5377 ,  A61K31/4439 ,  A61K31/428 ,  A61K31/433 ,  A61K31/422 ,  C07D249/12 ,  C07D417/10 ,  C07D405/12 ,  C07D403/12 ,  C07D401/04 ,  C07D403/04 ,  C07D403/10 ,  C07D409/14 ,  C07D417/12 ,  C07D413/10

CPC classification number: A61K31/4196 ,  A61K31/422 ,  A61K31/4245 ,  A61K31/428 ,  A61K31/433 ,  A61K31/4439 ,  A61K31/5377 ,  C07D249/12 ,  C07D401/04 ,  C07D401/10 ,  C07D403/04 ,  C07D403/10 ,  C07D403/12 ,  C07D405/12 ,  C07D409/14 ,  C07D413/10 ,  C07D413/12 ,  C07D417/10 ,  C07D417/12

Abstract: The present disclosure is directed to compounds of formula (I), and pharmaceutically acceptable salts thereof, as mPGES-1 inhibitors. These compounds are inhibitors of the microsomal prostaglandin E synthase-1 (mPGES-1) enzyme and are therefore useful in the treatment of pain and/or inflammation from a variety of diseases or conditions, such as asthma, osteoarthritis, rheumatoid arthritis, acute or chronic pain and neurodegenerative diseases.

公开(公告)号：US20180134671A1

公开(公告)日：2018-05-17

申请号：US15573387

申请日：2016-06-13

Applicant: Glenmark Pharmaceuticals S.A.

Inventor： Nagarajan Muthukaman ,  Laxmikant A. Gharat ,  Suresh M. Kadam ,  Sachin Gavhane ,  Sandeep B. Khandagale ,  Sunil P. Nirgude

IPC: C07D249/12 ,  A61P29/00

CPC classification number: C07D249/12 ,  A61P29/00 ,  G01N23/20075 ,  G01N2021/3595

Abstract: The present application relates to solid state forms of a triazolone compound which exhibit mPGES-1 enzyme inhibition activity, specifically N-(4-chloro-3-(5-oxo-1-(4-(trifluoromethyl)phenyl)-4,5-dihydro-1H-1,2,4-triazol-3-yl)benzyl) pivalamide (Compound of formula II), and process for preparation thereof.

公开(公告)号：US20160339000A1

公开(公告)日：2016-11-24

申请号：US15228681

申请日：2016-08-04

Applicant: Glenmark Pharmaceuticals S.A.

Inventor： Laxmikant A. Gharat ,  Nagarajan Muthukaman ,  Neelima Khairatkar-Joshi ,  Vidya G. Kattige

IPC: A61K31/4196 ,  A61K31/5377 ,  A61K31/422 ,  A61K31/428 ,  A61K31/433 ,  A61K31/4439 ,  A61K31/4245

CPC classification number: A61K31/4196 ,  A61K31/422 ,  A61K31/4245 ,  A61K31/428 ,  A61K31/433 ,  A61K31/4439 ,  A61K31/5377 ,  C07D249/12 ,  C07D401/04 ,  C07D401/10 ,  C07D403/04 ,  C07D403/10 ,  C07D403/12 ,  C07D405/12 ,  C07D409/14 ,  C07D413/10 ,  C07D413/12 ,  C07D417/10 ,  C07D417/12

Abstract: The present disclosure is directed to compounds of formula (I), and pharmaceutically acceptable salts thereof, as mPGES-1 inhibitors. These compounds are inhibitors of the microsomal prostaglandin E synthase-1 (mPGES-1) enzyme and are therefore useful in the treatment of pain and/or inflammation from a variety of diseases or conditions, such as asthma, osteoarthritis, rheumatoid arthritis, acute or chronic pain and neurodegenerative diseases.

公开(公告)号：US20190282548A1

公开(公告)日：2019-09-19

申请号：US16423992

申请日：2019-05-28

Applicant: Glenmark Pharmaceuticals S.A.

Inventor： Laxmikant A. Gharat ,  Nagarajan Muthukaman ,  Neelima Khairatkar-Joshi ,  Vidya G. Kattige

IPC: A61K31/4196 ,  A61K31/4245 ,  C07D401/10 ,  A61K31/5377 ,  A61K31/4439 ,  A61K31/428 ,  A61K31/433 ,  A61K31/422 ,  C07D249/12 ,  C07D417/10 ,  C07D405/12 ,  C07D403/12 ,  C07D401/04 ,  C07D403/04 ,  C07D403/10 ,  C07D409/14 ,  C07D417/12 ,  C07D413/10 ,  C07D413/12

Abstract: The present disclosure is directed to compounds of formula (I), and pharmaceutically acceptable salts thereof, as mPGES-1 inhibitors. These compounds are inhibitors of the microsomal prostaglandin E synthase-1 (mPGES-1) enzyme and are therefore useful in the treatment of pain and/or inflammation from a variety of diseases or conditions, such as asthma, osteoarthritis, rheumatoid arthritis, acute or chronic pain and neurodegenerative diseases.

公开(公告)号：US10112914B2

公开(公告)日：2018-10-30

申请号：US15573387

申请日：2016-06-13

Applicant: Glenmark Pharmaceuticals S.A.

Inventor： Nagarajan Muthukaman ,  Laxmikant A. Gharat ,  Suresh M. Kadam ,  Sachin Gavhane ,  Sandeep B. Khandagale ,  Sunil P. Nirgude

IPC: C07D249/12 ,  A61P29/00 ,  G01N23/20 ,  G01N21/35

Abstract: The present application relates to solid state forms of a triazolone compound which exhibit mPGES-1 enzyme inhibition activity, specifically N-(4-chloro-3-(5-oxo-1-(4-(trifluoromethyl)phenyl)-4,5-dihydro-1H-1,2,4-triazol-3-yl)benzyl) pivalamide (Compound of formula II), and process for preparation thereof.

公开(公告)号：US10457649B2

公开(公告)日：2019-10-29

申请号：US16119306

申请日：2018-08-31

Applicant: Glenmark Pharmaceuticals S.A.

Inventor： Nagarajan Muthukaman ,  Laxmikant A. Gharat ,  Suresh M. Kadam ,  Sachin Gavhane ,  Sandeep B. Khandagale ,  Sunil P. Nirgude

IPC: C07D249/12 ,  A61P29/00 ,  G01N23/20 ,  G01N21/35

Abstract: The present application relates to solid state forms of a triazolone compound which exhibit mPGES-1 enzyme inhibition activity, specifically N-(4-chloro-3-(5-oxo-1-(4-(trifluoromethyl)phenyl)-4,5-dihydro-1H-1,2,4-triazol-3-yl)benzyl)pivalamide (Compound of formula II), and process for preparation thereof.

公开(公告)号：US10391083B2

公开(公告)日：2019-08-27

申请号：US15919460

申请日：2018-03-13

Applicant: Glenmark Pharmaceuticals S.A.

Inventor： Laxmikant A. Gharat ,  Nagarajan Muthukaman ,  Neelima Khairatkar-Joshi ,  Vidya G. Kattige

IPC: C07D249/12 ,  A61K31/4196 ,  A61K31/4245 ,  A61K31/428 ,  A61K31/433 ,  A61K31/4439 ,  A61K31/5377 ,  C07D401/04 ,  C07D401/10 ,  C07D403/04 ,  C07D403/10 ,  C07D403/12 ,  C07D405/12 ,  C07D409/14 ,  C07D413/10 ,  C07D413/12 ,  C07D417/10 ,  C07D417/12 ,  A61K31/422

Abstract: The present disclosure is directed to compounds of formula (I), and pharmaceutically acceptable salts thereof, as mPGES-1 inhibitors. These compounds are inhibitors of the microsomal prostaglandin E synthase-1 (mPGES-1) enzyme and are therefore useful in the treatment of pain and/or inflammation from a variety of diseases or conditions, such as asthma, osteoarthritis, rheumatoid arthritis, acute or chronic pain and neurodegenerative diseases.

公开(公告)号：US20180370923A1

公开(公告)日：2018-12-27

申请号：US16119306

申请日：2018-08-31

Applicant: Glenmark Pharmaceuticals S.A.

Inventor： Nagarajan Muthukaman ,  Laxmikant A. Gharat ,  Suresh M. Kadam ,  Sachin Gavhane ,  Sandeep B. Khandagale ,  Sunil P. Nirgude

IPC: C07D249/12 ,  A61P29/00 ,  G01N21/35 ,  G01N23/20

CPC classification number: C07D249/12 ,  A61P29/00 ,  G01N23/20075 ,  G01N2021/3595

Abstract: The present application relates to solid state forms of a triazolone compound which exhibit mPGES-1 enzyme inhibition activity, specifically N-(4-chloro-3-(5-oxo-1-(4-(trifluoromethyl)phenyl)-4,5-dihydro-1H-1,2,4-triazol-3-yl)benzyl) pivalamide (Compound of formula II), and process for preparation thereof.

公开(公告)号：US09949955B2

公开(公告)日：2018-04-24

申请号：US15228681

申请日：2016-08-04

Applicant: Glenmark Pharmaceuticals S.A.

Inventor： Laxmikant A. Gharat ,  Nagarajan Muthukaman ,  Neelima Khairatkar-Joshi ,  Vidya G. Kattige

IPC: A61K31/4196 ,  A61K31/4245 ,  A61K31/428 ,  A61K31/433 ,  A61K31/4439 ,  A61K31/5377 ,  C07D249/12 ,  C07D401/04 ,  C07D401/10 ,  C07D403/04 ,  C07D403/10 ,  C07D403/12 ,  C07D405/12 ,  C07D409/14 ,  C07D413/10 ,  C07D413/12 ,  C07D417/10 ,  C07D417/12 ,  A61K31/422

CPC classification number: A61K31/4196 ,  A61K31/422 ,  A61K31/4245 ,  A61K31/428 ,  A61K31/433 ,  A61K31/4439 ,  A61K31/5377 ,  C07D249/12 ,  C07D401/04 ,  C07D401/10 ,  C07D403/04 ,  C07D403/10 ,  C07D403/12 ,  C07D405/12 ,  C07D409/14 ,  C07D413/10 ,  C07D413/12 ,  C07D417/10 ,  C07D417/12

Abstract: The present disclosure is directed to compounds of formula (I), and pharmaceutically acceptable salts thereof, as mPGES-1 inhibitors. These compounds are inhibitors of the microsomal prostaglandin E synthase-1 (mPGES-1) enzyme and are therefore useful in the treatment of pain and/or inflammation from a variety of diseases or conditions, such as asthma, osteoarthritis, rheumatoid arthritis, acute or chronic pain and neurodegenerative diseases.