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公开(公告)号：US10821100B2
公开(公告)日：2020-11-03
申请号：US16423992
申请日：2019-05-28
IPC分类号： 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
摘要： 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.
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公开(公告)号：US20180237428A1
公开(公告)日：2018-08-23
申请号：US15956168
申请日：2018-04-18
发明人： 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分类号： 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分类号： 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
摘要： 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.
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公开(公告)号：US10758517B2
公开(公告)日：2020-09-01
申请号：US16282125
申请日：2019-02-21
发明人： Monika Tandon , Sumit Sant , Neelima Khairatkar-Joshi , Girish Gudi , Vinu C. A. Menon , Ravi Talluri
IPC分类号： A61K31/4196 , A61P19/02 , A61K9/16 , A61K9/00 , A61K9/14
摘要： The present invention relates to a microsomal prostaglandin E synthases-1 (“mPGES-1”) inhibitor for the treatment of osteoarthritis pain in a subject. For example, the present invention relates to a method of treating moderate osteoarthritis pain in a subject in need thereof by orally administering to the subject a substituted triazolone compound as a mPGES-1 inhibitor. The present invention also relates to pharmaceutical compositions comprising the mPGES-1 inhibitor, and to processes for preparing such pharmaceutical compositions.
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公开(公告)号：US10391083B2
公开(公告)日：2019-08-27
申请号：US15919460
申请日：2018-03-13
IPC分类号： 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
摘要： 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.
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公开(公告)号：US10336688B2
公开(公告)日：2019-07-02
申请号：US16204977
申请日：2018-11-29
发明人： 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分类号： C07C237/42 , A61P11/14 , A61P11/08 , A61P17/06 , A61P11/06
摘要： 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.
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公开(公告)号：US10189775B2
公开(公告)日：2019-01-29
申请号：US15754037
申请日：2016-08-26
发明人： 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分类号： C07C237/42 , A61P11/06 , A61P11/08 , A61P11/14 , A61P17/06
摘要： 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.
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公开(公告)号：US09006257B2
公开(公告)日：2015-04-14
申请号：US13761937
申请日：2013-02-07
发明人： Laxmikant Atmaram Gharat , Abhisek Banerjee , Neelima Khairatkar-Joshi , Vidya Ganapati Kattige
IPC分类号： A01N43/54 , A61K31/517 , C07D239/88 , C07D215/233 , C07D239/94 , C07D401/12 , C07D217/22 , C07D217/24
CPC分类号： C07D239/88 , C07D215/233 , C07D217/22 , C07D217/24 , C07D239/94 , C07D401/12
摘要： 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.
摘要翻译： 本公开涉及作为mPGES-1抑制剂的式（I）化合物及其药学上可接受的盐。 这些化合物是微粒体前列腺素E合酶-1（mPGES-1）酶的抑制剂，因此可用于治疗各种疾病或病症如哮喘，骨关节炎，类风湿性关节炎，急性或类风湿性关节炎的疼痛和/或炎症 慢性疼痛和神经退行性疾病。
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公开(公告)号：US20230000872A1
公开(公告)日：2023-01-05
申请号：US17821379
申请日：2022-08-22
IPC分类号： A61K31/519 , A61K31/381 , A61K31/165 , A61K31/195 , A61P29/02 , A61K9/00
摘要： The present patent application relates to a transient receptor potential ankyrin-1 (“TRPA1”) antagonist for the treatment of neuropathic pain in a subject. Particularly, the present patent application relates to a method of treating neuropathic pain in a subject in need thereof by orally administering to the subject a thienopyrimidinedione Compound as a TRPA1 antagonist. The present invention also relates to a pharmaceutical composition comprising the TRPA1 antagonist, and a process for preparing such a pharmaceutical composition.
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公开(公告)号：US10344024B2
公开(公告)日：2019-07-09
申请号：US15956168
申请日：2018-04-18
发明人： 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分类号： 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
摘要： 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.
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公开(公告)号：US20180200229A1
公开(公告)日：2018-07-19
申请号：US15919460
申请日：2018-03-13
IPC分类号： 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分类号： 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
摘要： 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.
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