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公开(公告)号：US09682977B2
公开(公告)日：2017-06-20
申请号：US15103658
申请日：2014-12-09
发明人： Sanjib Das , Sachin Sundarlal Chaudhari , Abraham Thomas , Shailesh Ramesh Pardeshi , Vishal Govindrao Deshmukh , Prashant Dilip Wadekar , Neelima Khairatkar-Joshi , Daisy Manish Shah , Malini Bajpai
IPC分类号： C07D231/56 , C07D401/04 , C07D209/12 , C07D471/04
CPC分类号： C07D471/04 , C07D209/12 , C07D231/56 , C07D401/04
摘要： The present disclosure is directed to compounds of formula (I) and pharmaceutically acceptable salts thereof, wherein X, X1, M, R2, R3, R4, R5, m, n, 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, neurodegenerative diseases and cancer.
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公开(公告)号：US20160339000A1
公开(公告)日：2016-11-24
申请号：US15228681
申请日：2016-08-04
IPC分类号： A61K31/4196 , A61K31/5377 , A61K31/422 , A61K31/428 , A61K31/433 , A61K31/4439 , A61K31/4245
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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公开(公告)号：US09073955B2
公开(公告)日：2015-07-07
申请号：US14058536
申请日：2013-10-21
发明人： Sukeerthi Kumar , Abraham Thomas , Sachin Sundarlal Chaudhari , Bipin Parsottam Kansagra , Venkata Ramana Yemireddy , Neelima Khairatkar-Joshi , Indranil Mukhopadhyay , Girish Gudi
IPC分类号： A61K31/535 , A61K31/519 , A61K31/425 , C07F9/6561 , C07D487/04 , C07D491/04 , C07D495/04 , C07D513/04 , C07D491/048
CPC分类号： C07F9/6561 , C07D487/04 , C07D491/04 , C07D491/048 , C07D495/04 , C07D513/04 , C07F9/65616
摘要： The present invention is related to 2-amino-4-arylthiazole derivatives as TRPA (Transient Receptor Potential subfamily A) modulators. In particular, compounds described herein are useful for treating or preventing diseases, conditions and/or disorders modulated by TRPA1 (Transient Receptor Potential subfamily A, member 1). Also provided herein are processes for preparing compounds described herein, intermediates used in their synthesis, pharmaceutical compositions thereof, and methods for treating or preventing diseases, conditions and/or disorders modulated by TRPA1.
摘要翻译： 本发明涉及作为TRPA（瞬时受体电位亚族A）调节剂的2-氨基-4-芳基噻唑衍生物。 特别地，本文所述的化合物可用于治疗或预防由TRPA1（瞬时受体电位亚科A，成员1）调节的疾病，病症和/或病症。 本文还提供了制备本文所述化合物的方法，其合成中使用的中间体，其药物组合物，以及用于治疗或预防由TRPA1调节的疾病，病症和/或障碍的方法。
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公开(公告)号：US09000159B2
公开(公告)日：2015-04-07
申请号：US14079932
申请日：2013-11-14
发明人： Sachin Sundarlal Chaudhari , Sukeerthi Kumar , Abraham Thomas , Nisha Parag Patil , Ashok Bhausaheb Kadam , Vishal Govindrao Deshmukh , Sachin Vasantrao Dhone , Rajendra Prakash Chikhale , Neelima Khairatkar-Joshi , Indranil Mukhopadhyay
IPC分类号： C07D487/00 , C07D487/04
CPC分类号： C07D487/04
摘要： The invention described herein relates to novel fused pyrimidinediones derivatives of formula (I) which are TRPA (Transient Receptor Potential subfamily A) modulators. In particular, compounds described herein are useful for treating or preventing diseases, conditions and/or disorders modulated by TRPA1 (Transient Receptor Potential subfamily A, member 1). This invention also provides processes for preparing compounds described herein, intermediates used in their synthesis, pharmaceutical compositions thereof, and methods for treating or preventing diseases, conditions and/or disorders modulated by TRPA1.
摘要翻译： 本文描述的发明涉及式（I）的新型稠合嘧啶二酮衍生物，其是TRPA（瞬时受体电位亚族A）调节剂。 特别地，本文所述的化合物可用于治疗或预防由TRPA1（瞬时受体电位亚科A，成员1）调节的疾病，病症和/或病症。 本发明还提供了制备本文所述化合物的方法，其合成中使用的中间体，其药物组合物，以及用于治疗或预防由TRPA1调节的疾病，病症和/或障碍的方法。
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15.发明申请FUSED PYRIMIDINE-DIONE DERIVATIVES AS TRPA1 MODULATORS 有权作为TRPA1调节剂的FUSED PYRIMININE-DIONE DERIVATIVES公开(公告)号：US20140128603A1
公开(公告)日：2014-05-08
申请号：US14079932
申请日：2013-11-14
发明人： Sachin Sundarlal Chaudhari , Sukeerthi Kumar , Abraham Thomas , Nisha Parag Patil , Ashok Bhausaheb Kadam , Vishal Govindrao Deshmukh , Sachin Vasantrao Dhone , Rajendra Prakash Chikhale , Neelima Khairatkar-Joshi , Indranil Mukhopadhyay
IPC分类号： C07D487/04
CPC分类号： C07D487/04
摘要： The invention described herein relates to novel fused pyrimidinediones derivatives of formula (I) which are TRPA (Transient Receptor Potential subfamily A) modulators. In particular, compounds described herein are useful for treating or preventing diseases, conditions and/or disorders modulated by TRPA1 (Transient Receptor Potential subfamily A, member 1). This invention also provides processes for preparing compounds described herein, intermediates used in their synthesis, pharmaceutical compositions thereof, and methods for treating or preventing diseases, conditions and/or disorders modulated by TRPA1.
摘要翻译： 本文描述的发明涉及式（I）的新型稠合嘧啶二酮衍生物，其是TRPA（瞬时受体电位亚族A）调节剂。 特别地，本文所述的化合物可用于治疗或预防由TRPA1（瞬时受体电位亚科A，成员1）调节的疾病，病症和/或病症。 本发明还提供了制备本文所述化合物的方法，其合成中使用的中间体，其药物组合物，以及用于治疗或预防由TRPA1调节的疾病，病症和/或障碍的方法。
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公开(公告)号：US20140051667A1
公开(公告)日：2014-02-20
申请号：US14058536
申请日：2013-10-21
发明人： Sukeerthi Kumar , Abraham Thomas , Sachin Sundarlal Chaudhari , Bipin Parsottam Kansagra , Venkata Ramana Yemireddy , Neelima Khairatkar-Joshi , Indranil Mukhopadhyay , Girish Gudi
IPC分类号： C07F9/6561
CPC分类号： C07F9/6561 , C07D487/04 , C07D491/04 , C07D491/048 , C07D495/04 , C07D513/04 , C07F9/65616
摘要： The present invention is related to 2-amino-4-arylthiazole derivatives as TRPA (Transient Receptor Potential subfamily A) modulators. In particular, compounds described herein are useful for treating or preventing diseases, conditions and/or disorders modulated by TRPA1 (Transient Receptor Potential subfamily A, member 1). Also provided herein are processes for preparing compounds described herein, intermediates used in their synthesis, pharmaceutical compositions thereof, and methods for treating or preventing diseases, conditions and/or disorders modulated by TRPA1.
摘要翻译： 本发明涉及作为TRPA（瞬时受体电位亚族A）调节剂的2-氨基-4-芳基噻唑衍生物。 特别地，本文所述的化合物可用于治疗或预防由TRPA1（瞬时受体电位亚科A，成员1）调节的疾病，病症和/或病症。 本文还提供了制备本文所述化合物的方法，其合成中使用的中间体，其药物组合物，以及用于治疗或预防由TRPA1调节的疾病，病症和/或障碍的方法。
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公开(公告)号：US20130210844A1
公开(公告)日：2013-08-15
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： C07D239/88 , C07D239/94 , C07D215/233 , C07D401/12
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：US10988467B2
公开(公告)日：2021-04-27
申请号：US16402948
申请日：2019-05-03
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 , C07D401/04 , C07D403/04 , C07D417/12 , C07D231/12 , C07D239/26 , C07D239/36 , C07D239/42 , C07D413/04 , C07D413/12 , C07D213/40 , C07D241/12 , C07D241/20 , 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：US20200247800A1
公开(公告)日：2020-08-06
申请号：US16610351
申请日：2018-05-04
发明人： Sukeerthi Kumar , Abraham Thomas , Sachin Sundarlal Chaudhari , Laxmikant Atmaram Gharat , Neelima Khairatkar-Joshi , Daisy Manish Shah , Indranil Mukhopadhyay
IPC分类号： C07D471/04
摘要： The present application relates to substituted fused heteroaryl and hetero-cyclic compounds, useful as nicotinamide adenine dinucleotide phosphate oxidase inhibitors (NADPH oxidase inhibitors), processes for their preparation, pharmaceutical compositions comprising the compounds, and the use of the compounds or the compositions in the treatment or prevention of various diseases, conditions and/or disorders mediated by NADPH oxidase. (Formula I)
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公开(公告)号：US20190282548A1
公开(公告)日：2019-09-19
申请号：US16423992
申请日：2019-05-28
IPC分类号： 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
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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