- PREPARATION OF 2-[2-METHYL-1-[[4-METHYLSULFONYL-2-(TRIFLUORO METHYL)PHENYL]METHYL] PYRROLO[2,3-B]PYRIDIN-3-YL]ACETIC ACID
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The present invention relates to a novel compound of Formula IV and use of said compound for the preparation of 2-[2-methyl-1-[[4-methylsulfonyl-2-(trifluoromethyl)phenyl] methyl]pyrrolo[2,3-b]pyridine-3-yl]acetic acid [fevipiprant], Formula IV wherein A is SO2Me, halogen or a leaving group. The present invention further relates to a process of preparation of pharmaceutical acceptable salts of fevipiprant and composition thereof.
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- Fevipiprant selective prostaglandin DP2 (CRTh2) inhibitor treatment of asthma
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Prostaglandin D2 (PGD2), a major prostanoid, releases from activated mast cells. It activates and recruits various inflammatory cells like eosinophils and basophils through DP2 receptors to the site of inflammation and further promotes late-phase allergic reactions. For the last decade, the scientific community has extensively explored this pathway and synthesized various specific DP2 receptor antagonists for the management of asthma. About 20 compounds with DP2 antagonistic activity have reached different stages of clinical development. Among these, fevipiprant is one of the most advanced oral DP2 inhibitors as it selectively blocks the DP2 receptors. Fevipiprant has demonstrated an acceptable safety profile in phase II studies as evident from significant reduction of moderate to severe asthma exacerbations. Currently this novel antiasthmatic drug is in phase III clinical trials. This review provides a brief overview of PGD2 blockers, particularly fevipiprant and its preclinical pharmacology and clinical development, by providing a summary of completed or ongoing clinical studies assessing its safety and efficacy in asthma.
- Singh,Saroj,Kumar,Kuhad,Kuhad
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p. 565 - 572
(2018/09/11)
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- Discovery of Fevipiprant (NVP-QAW039), a Potent and Selective DP2 Receptor Antagonist for Treatment of Asthma
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Further optimization of an initial DP2 receptor antagonist clinical candidate NVP-QAV680 led to the discovery of a follow-up molecule 2-(2-methyl-1-(4-(methylsulfonyl)-2-(trifluoromethyl)benzyl)-1H-pyrrolo[2,3-b]pyridin-3-yl)acetic acid (compou
- Sandham, David A.,Barker, Lucy,Brown, Lyndon,Brown, Zarin,Budd, David,Charlton, Steven J.,Chatterjee, Devnandan,Cox, Brian,Dubois, Gerald,Duggan, Nicholas,Hall, Edward,Hatto, Julia,Maas, Janet,Manini, Jodie,Profit, Rachael,Riddy, Darren,Ritchie, Catherine,Sohal, Bindi,Shaw, Duncan,Stringer, Rowan,Sykes, David A.,Thomas, Matthew,Turner, Katharine L.,Watson, Simon J.,West, Ryan,Willard, Elisabeth,Williams, Gareth,Willis, Jennifer
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p. 582 - 586
(2017/05/17)
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- SUBSTITUTED AMINOTHIAZOLONE INDAZOLES AS ESTROGEN RELATED RECEPTOR-ALPHA MODULATORS
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The present invention relates to compounds of Formula (I), methods for preparing these compounds, compositions, intermediates and derivatives thereof and for treating a condition including but not limited to ankylosing spondylitis, artherosclerosis, arthritis (such as rheumatoid arthritis, infectious arthritis, childhood arthritis, psoriatic arthritis, reactive arthritis), bone-related diseases (including those related to bone formation), breast cancer (including those unresponsive to anti-estrogen therapy), cardiovascular disorders, cartilage-related disease (such as cartilage injury/loss, cartilage degeneration, and those related to cartilage formation), chondrodysplasia, chondrosarcoma, chronic back injury, chronic bronchitis, chronic inflammatory airway disease, chronic obstructive pulmonary disease, diabetes, disorders of energy homeostasis, gout, pseudogout, lipid disorders, metabolic syndrome, multiple myeloma, obesity, osteoarthritis, osteogenesis imperfecta, osteolytic bone metastasis, osteomalacia, osteoporosis, Paget's disease, periodontal disease, polymyalgia rheumatica, Reiter's syndrome, repetitive stress injury, hyperglycemia, elevated blood glucose level, and insulin resistance.
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- AMINOTHIAZOLONES AS ESTROGEN RELATED RECEPTOR-ALPHA MODULATORS
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The present invention relates to compounds of Formula (I), methods for preparing these compounds, compositions, intermediates and derivatives thereof and for treating a condition including but not limited to ankylosing spondylitis, artherosclerosis, arthritis (such as rheumatoid arthritis, infectious arthritis, childhood arthritis, psoriatic arthritis, reactive arthritis), bone-related diseases (including those related to bone formation), breast cancer (including those unresponsive to anti-estrogen therapy), cardiovascular disorders, cartilage-related disease (such as cartilage injury/loss, cartilage degeneration, and those related to cartilage formation), chondrodysplasia, chondrosarcoma, chronic back injury, chronic bronchitis, chronic inflammatory airway disease, chronic obstructive pulmonary disease, diabetes, disorders of energy homeostasis, gout, pseudogout, lipid disorders, metabolic syndrome, multiple myeloma, obesity, osteoarthritis, osteogenesis imperfecta, osteolytic bone metastasis, osteomalacia, osteoporosis, Paget's disease, periodontal disease, polymyalgia rheumatica, Reiter's syndrome, repetitive stress injury, hyperglycemia, elevated blood glucose level, and insulin resistance.
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- USE OF PYRROLO [2 , 3-B] PYRIDINES TO PREPARE A MEDICAMENT FOR TREATING PAIN
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There are provided according to the invention compounds of formula (I), in free or salt form, wherein R1, R2, R3, R4, R5, R6, Q, W, X, m, n and p are as described in the specification, process for preparing them, and their use in the manufacture of a medicament for the treatment of neuropathic pain.
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Page/Page column 55
(2008/06/13)
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- ORGANIC COMPOUNDS
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There are provided according to the invention compounds of formula (I) in free or salt form, wherein R1, R2, R4, R5, R6, D, X, W, m and n are as described in the specification, process for preparing t
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Page/Page column 24
(2008/06/13)
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- ORGANIC COMPOUNDS
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There are provided according to the invention compounds of formula (I), in free or salt form, wherein R1, R2, R3, R4, R5, R6, Q, W, X, m, n and p are as described in the specification, process for preparing them, and their use as pharmaceuticals.
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Page/Page column 60
(2010/02/15)
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