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：US20180237428A1

公开(公告)日：2018-08-23

申请号：US15956168

申请日：2018-04-18

Applicant: Glenmark Pharmaceuticals S.A.

Inventor： Sanjib Das ,  Laxmikant A. Gharat ,  Rajendra L. Harde ,  Sandeep Y. Shelke ,  Shailesh R. Pardeshi ,  Abraham Thomas ,  Neelima Khairatkar-Joshi ,  Daisy M. Shah ,  Malini Bajpai

IPC: C07D417/12 ,  C07D213/40 ,  C07D413/12 ,  C07D413/04 ,  C07D239/42 ,  C07D239/36 ,  C07D241/18 ,  C07D403/04 ,  C07D401/04 ,  C07D231/12 ,  C07D405/14 ,  C07D241/20 ,  C07D241/12 ,  C07D239/26

CPC classification number: C07D417/12 ,  C07D213/40 ,  C07D231/12 ,  C07D239/26 ,  C07D239/36 ,  C07D239/42 ,  C07D241/12 ,  C07D241/18 ,  C07D241/20 ,  C07D401/04 ,  C07D403/04 ,  C07D405/14 ,  C07D413/04 ,  C07D413/12

Abstract: The present disclosure is directed to compounds of formula (I) and pharmaceutically acceptable salts thereof, wherein ring A, ring B, L, R1, R2, R3, R4, R5, Ra, Rb, n, m, p and q are as defined herein, which are active as modulators of retinoid-related Sorphan receptor gamma t (RORγt). These compounds prevent, inhibit, or suppress the action of RORγt and are therefore useful in the treatment of RORγt mediated diseases, disorders, syndromes or conditions such as, e.g., pain, inflammation, COPD, asthma, rheumatoid arthritis, colitis, multiple sclerosis, psoriasis, neurodegenerative diseases and cancer.

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：US10336688B2

公开(公告)日：2019-07-02

申请号：US16204977

申请日：2018-11-29

Applicant: Glenmark Pharmaceuticals S.A.

Inventor： Sanjib Das ,  Laxmikant A. Gharat ,  Rajendra L. Harde ,  Dnyaneshwar E. Shelke ,  Shailesh R. Pardeshi ,  Abraham Thomas ,  Neelima Khairatkar-Joshi ,  Daisy M. Shah ,  Malini Bajpai

IPC: C07C237/42 ,  A61P11/14 ,  A61P11/08 ,  A61P17/06 ,  A61P11/06

Abstract: The present disclosure is directed to novel carbocyclic compounds of formula (I) and pharmaceutically acceptable salts thereof, wherein R1, R2, R3, R4, R5, R6, Ra, Rb, n, m and p are as defined herein, which are active as modulators of retinoid-related orphan receptor gamma t (RORγt). These compounds prevent, inhibit, or suppress the action of RORγt and are therefore useful in the treatment of RORγt mediated diseases, disorders, syndromes or conditions such as, e.g., pain, inflammation, COPD, asthma, rheumatoid arthritis, colitis, multiple sclerosis, psoriasis, neurodegenerative diseases and cancer.

公开(公告)号：US10189775B2

公开(公告)日：2019-01-29

申请号：US15754037

申请日：2016-08-26

Applicant: Glenmark Pharmaceuticals S.A.

Inventor： Sanjib Das ,  Laxmikant A. Gharat ,  Rajendra L. Harde ,  Dnyaneshwar E. Shelke ,  Shailesh R. Pardeshi ,  Abraham Thomas ,  Neelima Khairatkar-Joshi ,  Daisy M. Shah ,  Malini Bajpai

IPC: C07C237/42 ,  A61P11/06 ,  A61P11/08 ,  A61P11/14 ,  A61P17/06

Abstract: The present disclosure is directed to novel carbocyclic compounds of formula (I) and pharmaceutically acceptable salts thereof, wherein R1, R2, R3, R4, R5, R6, Ra, Rb, n, m and p are as defined herein, which are active as modulators of retinoid-related orphan receptor gamma t (RORγt). These compounds prevent, inhibit, or suppress the action of RORγt and are therefore useful in the treatment of RORγt mediated diseases, disorders, syndromes or conditions such as, e.g., pain, inflammation, COPD, asthma, rheumatoid arthritis, colitis, multiple sclerosis, psoriasis, neurodegenerative diseases and cancer.

公开(公告)号：US10344024B2

公开(公告)日：2019-07-09

申请号：US15956168

申请日：2018-04-18

Applicant: Glenmark Pharmaceuticals S.A.

Inventor： Sanjib Das ,  Laxmikant A. Gharat ,  Rajendra L. Harde ,  Sandeep Y. Shelke ,  Shailesh R. Pardeshi ,  Abraham Thomas ,  Neelima Khairatkar-Joshi ,  Daisy M. Shah ,  Malini Bajpai

IPC: C07D241/18 ,  C07D241/20 ,  C07D401/04 ,  C07D403/04 ,  C07D417/12 ,  C07D231/12 ,  C07D239/26 ,  C07D239/36 ,  C07D239/42 ,  C07D413/04 ,  C07D413/12 ,  C07D213/40 ,  C07D241/12 ,  C07D405/14

Abstract: The present disclosure is directed to compounds of formula (I) and pharmaceutically acceptable salts thereof, wherein ring A, ring B, L, R1, R2, R3, R4, R5, Ra, Rb, n, m, p and q are as defined herein, which are active as modulators of retinoid-related orphan receptor gamma t (RORγt). These compounds prevent, inhibit, or suppress the action of RORγt and are therefore useful in the treatment of RORγt mediated diseases, disorders, syndromes or conditions such as, e.g., pain, inflammation, COPD, asthma, rheumatoid arthritis, colitis, multiple sclerosis, psoriasis, neurodegenerative diseases and cancer.

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.