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Clofutriben

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Clofutriben

Cas 1204178-50-6

HCL 1203941-88-1

  • ASP 3662
  • 4-(5-(2-(4-Chloro-2,6-difluorophenoxy)propan-2-yl)-4-methyl-4H-1,2,4-triazol-3-yl)-3-fluorobenzamide
  • 4-{5-[2-(4-Chloro-2,6-difluorophenoxy)propan-2-yl]-4-methyl-4H-1,2,4-triazol-3-yl}-3-fluorobenzamide
  • 4-[5-[2-(4-chloro-2,6-difluorophenoxy)propan-2-yl]-4-methyl-1,2,4-triazol-3-yl]-3-fluorobenzamide
  • 4L1TY1U5VC
Molecular Weight424.80
FormulaC19H16ClF3N4O2

Clofutriben (ASP3662) is a 11β-hydroxysteroid dehydrogenase type 1 inhibitor.


Clofutriben is an orally bioavailable selective inhibitor of the enzyme 11beta-hydroxysteroid dehydrogenase type 1 (11b-HSD1; 11bHSD1; HSD11B1; HSD1; HSD-1), with potential protective activity for disorders of corticosteroid excess. Upon oral administration, clofutriben selectively binds to and inhibits the activity of HSD-1. This prevents the conversion of cortisone to the active hormone cortisol and thereby preventing the activation of the glucocorticoid receptors (GRs). By blocking cortisol production in metabolic tissues, clofutriben may inhibit the adverse metabolic effects that are caused by exogenous administration of glucocorticoids or in disorders in which cortisol is secreted in excess. HSD-1 is highly expressed in metabolic tissues, such as liver, skeletal muscle, and adipose tissue. It plays a crucial role in regulating the production of cortisol to activate the GRs.

SCHEME

PATENTS

Clinical and Translational Science (2019), 12(3), 291-301

British Journal of Pharmacology (2018), 175(19), 3784-3796

Sparrow Pharmaceuticals, Inc. WO2020106337

WO2019075394

WO2018117063

WO2010001946

PATENT

PDT PAT FOR HCL SALT, WO2012033070

https://patentscope.wipo.int/search/en/detail.jsf?docId=WO2012033070

PATENT

PDT PAT FOR BASE, WO2018117063

PATENT

WO2010001946 

[1]. Kiso T, et al. Analgesic effects of ASP3662, a novel 11尾-hydroxysteroid dehydrogenase 1 inhibitor, in rat models of neuropathic and dysfunctional pain. Br J Pharmacol. 2018 Oct;175(19):3784-3796.  [Content Brief]

////////////Clofutriben, ASP 3662, orphan drug, 4L1TY1U5VC, Sparrow Pharmaceuticals,


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DR ANTHONY CRASTO

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DR ANTHONY MELVIN CRASTO Ph.D

DR ANTHONY MELVIN CRASTO Ph.D

DR ANTHONY MELVIN CRASTO, Born in Mumbai in 1964 and graduated from Mumbai University, Completed his Ph.D from ICT, 1991,Matunga, Mumbai, India, in Organic Chemistry, The thesis topic was Synthesis of Novel Pyrethroid Analogues, Currently he is working with AFRICURE PHARMA, ROW2TECH, NIPER-G, Department of Pharmaceuticals, Ministry of Chemicals and Fertilizers, Govt. of India as ADVISOR, earlier assignment was with GLENMARK LIFE SCIENCES LTD, as CONSUlTANT, Retired from GLENMARK in Jan2022 Research Centre as Principal Scientist, Process Research (bulk actives) at Mahape, Navi Mumbai, India. Total Industry exp 32 plus yrs, Prior to joining Glenmark, he has worked with major multinationals like Hoechst Marion Roussel, now Sanofi, Searle India Ltd, now RPG lifesciences, etc. He has worked with notable scientists like Dr K Nagarajan, Dr Ralph Stapel, Prof S Seshadri, etc, He did custom synthesis for major multinationals in his career like BASF, Novartis, Sanofi, etc., He has worked in Discovery, Natural products, Bulk drugs, Generics, Intermediates, Fine chemicals, Neutraceuticals, GMP, Scaleups, etc, he is now helping millions, has 9 million plus hits on Google on all Organic chemistry websites. His friends call him Open superstar worlddrugtracker. His New Drug Approvals, Green Chemistry International, All about drugs, Eurekamoments, Organic spectroscopy international, etc in organic chemistry are some most read blogs He has hands on experience in initiation and developing novel routes for drug molecules and implementation them on commercial scale over a 32 PLUS year tenure till date Feb 2023, Around 35 plus products in his career. He has good knowledge of IPM, GMP, Regulatory aspects, he has several International patents published worldwide . He has good proficiency in Technology transfer, Spectroscopy, Stereochemistry, Synthesis, Polymorphism etc., He suffered a paralytic stroke/ Acute Transverse mylitis in Dec 2007 and is 90 %Paralysed, He is bound to a wheelchair, this seems to have injected feul in him to help chemists all around the world, he is more active than before and is pushing boundaries, He has 100 million plus hits on Google, 2.5 lakh plus connections on all networking sites, 100 Lakh plus views on dozen plus blogs, 227 countries, 7 continents, He makes himself available to all, contact him on +91 9323115463, email amcrasto@gmail.com, Twitter, @amcrasto , He lives and will die for his family, 90% paralysis cannot kill his soul., Notably he has 38 lakh plus views on New Drug Approvals Blog in 227 countries......https://newdrugapprovals.wordpress.com/ , He appreciates the help he gets from one and all, Friends, Family, Glenmark, Readers, Wellwishers, Doctors, Drug authorities, His Contacts, Physiotherapist, etc He has total of 32 International and Indian awards

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