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DRUG APPROVALS BY DR ANTHONY MELVIN CRASTO
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Milpecitinib
Milpecitinib
CAS 1415819-54-3
MF C20H20N4O2S MW380.5 g/mol
N-[3-[4-[5-(pyrrolidine-1-carbonyl)-1H-pyrrol-3-yl]-1,3-thiazol-2-yl]phenyl]acetamide
N-(3-{4-[5-(pyrrolidine-1-carbonyl)-1H-pyrrol-3-yl]-1,3-thiazol-2-yl}phenyl)acetamide
Janus tyrosine kinase inhibitor, anti-inflammatory, veterinary, PF-06263276, PF 06263276, Ph 1012, DNX 04013, CPh 1012, Ph-1012, CVXL 0074-02, 4Q8TT4B4GN
Milpecitinib is a small molecule drug. Milpecitinib has a monoisotopic molecular weight of 380.13 Da.
Milpecitinib (also known by its developmental codes PF-06263276, Ph-1012, and DNX-04013) is a potent, small-molecule Janus kinase (JAK) inhibitor used primarily in veterinary medicine and laboratory research. It functions as an ATP-competitive, broad-spectrum (pan-JAK) inhibitor that targets all four members of the JAK family: JAK1, JAK2, JAK3, and Tyrosine Kinase 2 (TYK2).
Primary Indication and Target
- Veterinary Use: Milpecitinib is designated for the control of pruritus (itching) associated with canine allergic dermatitis and the management of canine atopic dermatitis (CAD).
- Sponsorship: The United States Adopted Name (USAN) for this drug was officially adopted following sponsorship by Phibro Animal Health.
- Research Use: In laboratory settings, it is utilized to study complex inflammatory pathways, immune disorders, and certain cancers.
Mechanism of Action
Milpecitinib works by blocking the ATP-binding site of JAK enzymes. This inhibition halts the JAK-STAT signaling pathway, which plays a critical role in cellular responses to inflammatory cytokines. By blocking this cascade, the drug prevents the production and signaling of pro-inflammatory cytokines that cause severe itching and skin inflammation in dogs.
SYN
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References
- Compositions and methods for modulating kinasesPublication Number: JP-6054379-B2Priority Date: 2011-06-07Grant Date: 2016-12-27
- Compositions and methods for modulating a kinasePublication Number: EP-2718290-B1Priority Date: 2011-06-07Grant Date: 2016-05-04
- Compositions and methods for modulating a kinasePublication Number: CA-2837268-CPriority Date: 2011-06-07Grant Date: 2020-05-12
- Compositions and Methods for Modulating a KinasePublication Number: US-2012316148-A1Priority Date: 2011-06-07
- Compositions and methods for modulating a kinasePublication Number: EP-2718290-A2Priority Date: 2011-06-07
- Compositions and methods for modulating a kinasePublication Number: WO-2012172438-A9Priority Date: 2011-06-07
- Compositions and methods for modulating a kinasePublication Number: US-8937065-B2Priority Date: 2011-06-07Grant Date: 2015-01-20
- Compositions and methods for modulating kinasesPublication Number: JP-2014520108-APriority Date: 2011-06-07
- Compositions and methods for modulating a kinasePublication Number: WO-2012172438-A2Priority Date: 2011-06-07
- Compositions and methods to modulate a kinasePublication Number: ES-2585244-T3Priority Date: 2011-06-07Grant Date: 2016-10-04
- Compound for modulating a kinase
- Publication Number: BR-112013031121-B1
- Priority Date: 2011-06-07
//////////milpecitinib, anax labs, Janus tyrosine kinase inhibitor, anti-inflammatory, veterinary, PF-06263276, PF 06263276, Ph 1012, DNX 04013, CPh 1012, Ph-1012, CVXL 0074-02, 4Q8TT4B4GN
Lirucitinib
Lirucitinib
CAS 2458115-78-9
MF C16H25N5OS MW335.5 g/mol
N-[4-[(ethylsulfonimidoyl)methyl]cyclohexyl]-N-methyl-7H-pyrrolo[2,3-d]pyrimidin-4-amine
(R)-ethyl(imino)({trans-4-[methyl(7H-pyrrolo[2,3-d]pyrimidin-4-yl)amino]cyclohexyl}methyl)-λ6
-sulfanone
Janus tyrosine kinase inhibitor, anti-inflammatory, GGW101, GGW 101
Lirucitinib is a Janus kinase (JAK) inhibitor primarily known as a novel, Class I veterinary drug. It specifically targets the JAK1 enzyme to block itch-inducing (pruritic) and inflammation-causing cytokines in the body.
Core Information
- Primary Use: The drug is developed for veterinary medicine to treat acute and chronic pruritic (severe itch) skin diseases in dogs, which are commonly caused by allergies, parasites, or infections.
- Approval Status: It received a Class I New Veterinary Drug Certificate from the Ministry of Agriculture and Rural Affairs (MARA) in China.
- Human Medicine: As of 2026, there are no clinical indications or indications that Lirucitinib is being tested for use in humans.
- Chemical Profile: It is an orally active small molecule with the chemical formula C₁₆H₂₅N₅OS and acts specifically as the (R)-enantiomer of the compound.
SYN
11 (1.0 g, 2.04 mmol) (prepared in step 9), tetrahydrofuran/methanol (10 mL), and cesium carbonate (1.33 g, 4.08 mmol) were added into a 25 mL single-necked flask, refluxed for 12 h, concentrated, and poured into dichloromethane and saturated salt solution, the organic phase was dried with anhydrous sodium sulfate, concentrated, and subjected to a conventional preparation method and a chiral preparation method to obtain product A as a white solid (20 mg, yield: 2.9%), LC-MS: 336 [M+H]+, H 1-NMR: 1H NMR (400 MHz, DMSO) δ 11.61 (s, 1H), 8.09 (s, 1H), 7.13 (s, 1H), 6.54 (s, 1H), 4.67 (s, 1H), 3.90-3.83 (m, 1H), 3.17 (s, 3H), 3.06-2.93 (m, 4H), 2.12-2.01 (m, 3H), 1.73-1.70 (m, 4H), 1.31-1.22 (m, 5H) and product B as a white solid (25 mg, yield: 3.7%), LC-MS: 336 [M+H]+, H 1—NMR: 1H NMR (400 MHz, DMSO) δ 11.59 (s, 1H), 8.09 (s, 1H), 7.12 (dd, J=3.3, 2.6 Hz, 1H), 6.54 (s, 1H), 4.67 (s, 1H), 3.58 (s, 1H), 3.17 (s, 3H), 3.06-2.89 (m, 4H), 2.16-1.93 (m, 3H), 1.74-1.69 (m, 4H), 1.25-1.23 (m, 5H).
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WEBSITE https://www.anaxlab.com/
Discovery Solutions, Supporting the chemistry needs of clients in the Medical, Analytical and Bio Sciences
Development Solutions, Developing from Lab scale to PR&D, Kilo Scale-ups and Commercial Scales
SEE MORE………Integrated Solutions, Manufacturing Solutions, Products,
Can’t Find? Let’s Connect
Phone : +91 897704 2010 / +91 9177075735, Email : info@anaxlab.com
#MedicinalChemistry, #DrugDiscovery, #OrganicSynthesis, #ChemicalLibrary, #BuildingBlocks, #SARStudies, #ChemistryInnovation, #medchem, #Drugdevelopment, #Biotech, #Biotechnology, #AnaxLaboratories, #Pharma
AS ON FEB2026 4.574 LAKHS VIEWS ON BLOG WORLDREACH AVAILABLEFOR YOUR ADVERTISEMENT
join me on Linkedin
Anthony Melvin Crasto Ph.D – India | LinkedIn
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RESEARCHGATE
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PAT
- Jak inhibitor and preparation method thereforPublication Number: EP-3915989-B1Priority Date: 2019-01-30Grant Date: 2023-06-28
- Jak inhibitor and preparation method thereforPublication Number: US-2022106319-A1Priority Date: 2019-01-30
- Jak inhibitor and preparation method thereforPublication Number: WO-2020155931-A1Priority Date: 2019-01-30
- Jak inhibitor and preparation method thereforPublication Number: EP-3915989-A1Priority Date: 2019-01-30
/////////lirucitinib, anax labs, Janus tyrosine kinase inhibitor, anti-inflammatory, GGW101, GGW 101
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