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ACTIVE PHARMA INGREDIENTS

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Chemistry

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Also known as: 1263774-59-9, Jte-052, Jte-052a, Corectim, Leo 124249a, Leo 124249
Molecular Formula
C16H18N6O
Molecular Weight
310.35  g/mol
InChI Key
LOWWYYZBZNSPDT-ZBEGNZNMSA-N
FDA UNII
9L0Q8KK220

Delgocitinib
Delgocitinib is under investigation in clinical trial NCT03683719 (Phase 2b Dose-ranging Trial to Evaluate Delgocitinib Cream 1, 3, 8, and 20 Mg/g Compared to Delgocitinib Cream Vehicle Over a 16-week Treatment Period in Adult Subjects With Chronic Hand Eczema).
1 2D Structure

Delgocitinib

2 Identification
2.1 Computed Descriptors
2.1.1 IUPAC Name
3-[(3S,4R)-3-methyl-7-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1,7-diazaspiro[3.4]octan-1-yl]-3-oxopropanenitrile
2.1.2 InChI
InChI=1S/C16H18N6O/c1-11-8-22(13(23)2-5-17)16(11)4-7-21(9-16)15-12-3-6-18-14(12)19-10-20-15/h3,6,10-11H,2,4,7-9H2,1H3,(H,18,19,20)/t11-,16-/m0/s1
2.1.3 InChI Key
LOWWYYZBZNSPDT-ZBEGNZNMSA-N
2.1.4 Canonical SMILES
CC1CN(C12CCN(C2)C3=NC=NC4=C3C=CN4)C(=O)CC#N
2.1.5 Isomeric SMILES
C[C@H]1CN([C@]12CCN(C2)C3=NC=NC4=C3C=CN4)C(=O)CC#N
2.2 Other Identifiers
2.2.1 UNII
9L0Q8KK220
2.3 Synonyms
2.3.1 MeSH Synonyms

1. 1,6-diazaspiro(3.4)octane-1-propanenitrile, 3-methyl-beta-oxo-6-(7h-pyrrolo(2,3-d)pyrimidin-4-yl)-, (3s,4r)-

2. 3-((3s,4r)-3-methyl-6-(7h-pyrrolo(2,3-d)pyrimidin-4-yl)-1,6-diazaspiro(3.4)octan-1-yl)-3-oxopropanenitrile

3. Jte-052

2.3.2 Depositor-Supplied Synonyms

1. 1263774-59-9

2. Jte-052

3. Jte-052a

4. Corectim

5. Leo 124249a

6. Leo 124249

7. Leo-124249a

8. Leo-124249

9. Delgocitinib [usan]

10. 9l0q8kk220

11. 3-[(3s,4r)-3-methyl-7-(7h-pyrrolo[2,3-d]pyrimidin-4-yl)-1,7-diazaspiro[3.4]octan-1-yl]-3-oxopropanenitrile

12. 3-((3s,4r)-3-methyl-6-(7h-pyrrolo(2,3-d)pyrimidin-4-yl)-1,6-diazaspiro(3.4)octan-1-yl)-3-oxopropanenitrile

13. 3-[(3s,4r)-3-methyl-7-(7h-pyrrolo[2,3-d]pyrimidin-4-yl)-1,7-diazaspiro[3.4]octan-1-yl]-3-oxidanylidene-propanenitrile

14. Delgocitinibum

15. Corectim (tn)

16. 3-((3s,4r)-3-methyl-6-(7h-pyrrolo[2,3-d]pyrimidin-4-yl)-1,6-diazaspiro[3.4]octan-1-yl)-3-oxopropanenitrile

17. 3-[(3s,4r)-3-methyl-6-(7h-pyrrolo[2,3-d]pyrimidin-4-yl)-1,6-diazaspiro[3.4]octan-1-yl]-3-oxopropanenitrile

18. Ent-60

19. Delgocitinib (jan/usan)

20. Delgocitinib [inn]

21. Delgocitinib [jan]

22. Delgocitinib [who-dd]

23. Unii-9l0q8kk220

24. Gtpl9619

25. Jte052

26. Chembl4297507

27. Schembl12547007

28. Chebi:167600

29. Dtxsid401336933

30. Ex-a5577

31. Bdbm50545650

32. At24880

33. Leo-124249;jte-052

34. Bd178539

35. Hy-109053

36. Cs-0031558

37. D11046

38. A936874

39. 1,6-diazaspiro(3.4)octane-1-propanenitrile, 3-methyl-.beta.-oxo-6-(7h-pyrrolo(2,3-d)pyrimidin-4-yl)-, (3s,4r)-

40. 1,6-diazaspiro(3.4)octane-1-propanenitrile, 3-methyl-beta-oxo-6-(7h-pyrrolo(2,3-d)pyrimidin-4-yl)-, (3s,4r)-

41. Fhx

2.4 Create Date
2011-03-14
3 Chemical and Physical Properties
Molecular Weight 310.35 g/mol
Molecular Formula C16H18N6O
XLogP31.1
Hydrogen Bond Donor Count1
Hydrogen Bond Acceptor Count5
Rotatable Bond Count2
Exact Mass310.15420922 g/mol
Monoisotopic Mass310.15420922 g/mol
Topological Polar Surface Area88.9 Ų
Heavy Atom Count23
Formal Charge0
Complexity544
Isotope Atom Count0
Defined Atom Stereocenter Count2
Undefined Atom Stereocenter Count0
Defined Bond Stereocenter Count0
Undefined Bond Stereocenter Count0
Covalently Bonded Unit Count1
4 Drug and Medication Information
4.1 Drug Indication

Treatment of dermatitis and eczema


INTERMEDIATE SUPPLIERS

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CAS Number : 2491-20-5

End Use API : Delgocitinib

About The Company : Blue Jet Healthcare is a global, science-driven pharmaceutical company specializing in collaboration, development, and manufacturing of advanced pharmaceutical ...

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CAS Number : 36140-83-7

End Use API : Delgocitinib

About The Company : Sunway Pharm ltd provides high quality building blocks to the global pharmaceutical and bio-technology industry. Combining our chemistry expertise and our econo...

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DATA COMPILATION #PharmaFlow

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FDA okays 50 new drugs in 2024; BMS’ Cobenfy, Lilly’s Kisunla lead pack of breakthrough therapies
In 2024, the biopharma industry continued to advance on its robust trajectory of innovation. Though the US Food and Drug Administration’s Center for Drug Evaluation and Research (CDER) and the Center for Biologics Evaluation and Research (CBER) approved fewer drugs, there was a significant increase in medical breakthroughs.While the CDER approved 50 new drugs in 2024, as compared to 55 in 2023, the CBER granted 14 biologics approvals in 2024, down from 20 in 2023.The European Medicines Agency (EMA) approved 34 new therapies, up from 32 in 2023, while Health Canada granted 28 approvals, down from 38 in 2023.The year saw long-awaited treatments being approved in areas such as schizophrenia and Alzheimer’s disease in the second half (H2) of 2024. In H1 2024, drugs to treat metabolic dysfunction-associated steatohepatitis (MASH) and chronic obstructive pulmonary disease (COPD) had been granted FDA approvals.As the year drew to a close, FDA began approving drugs at a feverish pace, with 29 of the CDER’s 50 approvals coming in H2.Like most years, the landscape of drug approvals was dominated by oncology, with 15 of the 50 drugs (30 percent) approved targeting various forms of cancer. This was followed by dermatology and non-malignant hematology, each accounting for 12 percent of approvals. Notably, small molecules continued to dominate the market, making up for 64 percent of the new drug approvals, while 32 percent were proteins, including monoclonal and bi-specific antibodies. View New Drug Approvals in 2024 with Estimated Sales (Free Excel Available)Karuna-BMS’ schizophrenia drug, Lilly’s Alzheimer’s med, Neurocrine’s Crenessity dominate list of pathbreaking approvals in H2Out of the 50 new drugs approved in 2024, CDER identified 24 (48 percent) as first-in-class, showcasing novel mechanisms of action. The most anticipated approval of 2024 was Karuna and Bristol Myers Squibb’s Cobenfy, a groundbreaking treatment for schizophrenia. This fixed-dose combination of xanomeline and trospium chloride represents the first novel mechanism of action in decades for this debilitating psychiatric condition. Analysts forecast peak annual sales of over US$ 3.3 billion for Cobenfy. Eli Lilly’s Alzheimer’s drug Kisunla (donanemab) became the third amyloid-targeting antibody to gain FDA approval. Unlike its predecessors, Kisunla offers a unique limited-duration treatment regimen, allowing patients to discontinue therapy once amyloid levels in the brain drop below a certain threshold. Priced at approximately US$ 32,000 per year, it is positioned as a cost-effective alternative to existing treatments. Analysts estimate peak sales of US$ 2.4 billion for Kisunla.Crenessity (crinecerfont), developed by Neurocrine Biosciences, became the first FDA-approved treatment in decades for classic congenital adrenal hyperplasia (genetic conditions that affect the adrenal glands). Similarly, Vertex’s triple combination therapy of deutivacaftor, tezacaftor & vanzacaftor (Alyftrek) for cystic fibrosis represents a significant advancement in genetic disease treatment. Analysts forecast peak sales exceeding US$ 8.3 billion, underscoring the therapy’s potential to transform patient care.Meanwhile, Bridgebio’s Attruby (acoramidis hydrochloride) emerged as a promising treatment for cardiac amyloidosis, a life-threatening condition. View New Drug Approvals in 2024 with Estimated Sales (Free Excel Available) Roche’s Itovebi, Checkpoint’s Unloxcyt clinch FDA approvals in H2 2024; forecast to achieve blockbuster statusThe dominance of cancer drug approvals reflects the ongoing focus on targeted therapies, immuno-oncology, and precision medicine to improve outcomes for patients with hard-to-treat cancers.Among the year’s notable FDA approvals was Genentech’s Itovebi (inavolisib), another targeted therapy that treats hormone receptor-positive (HR+), HER2-negative breast cancer. Itovebi is a PI3Kα inhibitor designed specifically for patients with PIK3CA mutations, a common driver of resistance to endocrine therapy in breast cancer. It demonstrated a more tolerable safety profile. Roche projects Itovebi’s peak (annual) sales to reach CHF 2 billion (US$ 2.3 billion).Checkpoint Therapeutics’ Unloxcyt (cosibelimab) joined the crowded checkpoint inhibitor market as the eleventh PD-1/PD-L1-targeting monoclonal antibody approved by the FDA. It was granted approval for cutaneous squamous cell carcinoma (cSCC), an aggressive form of skin cancer with high recurrence rates. As compared to other checkpoint inhibitors, like Keytruda (pembrolizumab) and Opdivo (nivolumab), Unloxcyt is likely to offer an advantage in immune activation.FDA also approved Astellas’ Vyloy (zolbetuximab), a first-in-class monoclonal antibody for metastatic gastric and gastroesophageal junction (GEJ) adenocarcinoma. Analysts forecast peak sales of approximately US$ 850 million for Vyloy.Syndax Pharmaceuticals’ Revuforj (revumenib) was approved by FDA to treat a type of acute leukemia in both adults and children. This approval introduces a novel class of medications known as menin inhibitors. These agents are currently in clinical development for the treatment of genetically defined subsets of acute leukemia. These inhibitors function by preventing the activation of cancer growth-related proteins. View New Drug Approvals in 2024 with Estimated Sales (Free Excel Available) Potential blockbusters Lilly’s Ebglyss, Galderma’s Nemluvio lead advances in dermatologyEli Lilly’s Ebglyss (lebrikizumab) garnered significant attention. Approved by FDA for moderate-to-severe atopic dermatitis, this monoclonal antibody introduces a less burdensome dosing regimen compared to its competitors, with maintenance therapy required only once a month. This feature positions it as a potential contender to Dupixent (dupilumab), a market leader in atopic dermatitis. Ebglyss sales are forecast to reach US$ 1.9 billion by 2030.Galderma’s Nemluvio (nemolizumab) secured FDA approval for two indications in 2024 — prurigo nodularis (a chronic disorder of the skin) and moderate-to-severe atopic dermatitis in patients aged 12 years and older. As the first humanized IgG2 monoclonal antibody targeting the IL-31 receptor, Nemluvio directly inhibits the key driver of itch and inflammation in both these conditions. With its unique mechanism and broad dermatology potential, analysts forecast peak sales of approximately US$ 1.66 billion. Ebglyss and Nemluvio underscore the growing importance of biologics in dermatological care.Botanix Pharmaceuticals also made strides in dermatology by clinching an FDA approval for Sofdra (sofpironium) in June. The drug has been okayed for the treatment of primary axillary hyperhidrosis, a condition characterized by excessive sweating.Ascendis Pharma’s Yorvipath (palopegteriparatide), a therapy approved by FDA to treat hypoparathyroidism, is forecast to achieve blockbuster sales of US$ 1.8 billion by 2030, highlighting its potential to transform endocrine care. View New Drug Approvals in 2024 with Estimated Sales (Free Excel Available) Our viewOverall, 2024 was defined by its breakthrough drug approvals. The year also saw significant reduction in complete response letters (CRLs) — they dropped from 43 in 2023 to just 29 in 2024. This suggests improved industry preparedness and alignment with regulatory expectations.The new year began with the approval of Datroway (datopotamab deruxtecan) from AstraZeneca and Daiichi Sankyo, marking a significant advancement in oncology. Several other promising new drugs are coming up for FDA approval this year, such as J&J’s nipocalimab, Vertex Pharmaceuticals’ suzetrigine, Elevar Therapeutics’ rivoceranib/camrelizumab, Sanofi’s fitusiran and GSK’s gepotidacin. Hopefully, the momentum of breakthrough approvals will continue through 2025, political headwinds in the US notwithstanding. 

Impressions: 13873

https://www.pharmacompass.com/radio-compass-blog/fda-okays-50-new-drugs-in-2024-bms-cobenfy-lilly-s-kisunla-lead-pack-of-breakthrough-therapies

#PharmaFlow by PHARMACOMPASS
30 Jan 2025

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US Patents

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LEO PHARMA AS

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DELGOCITINIB

US Patent Number : 8609647

Drug Substance Claim : Y

Drug Product Claim : Y

Application Number : 219155

Patent Use Code : U-4237

Delist Requested :

Patent Use Description :

Patent Expiration Date : 2031-09-19

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US Exclusivities

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LEO PHARMA AS

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DELGOCITINIB

Exclusivity Code : NCE

Exclusivity Expiration Date : 2030-07-23

Application Number : 219155

Product Number : 1

Exclusivity Details :

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ABOUT THIS PAGE

Looking for 1263774-59-9 / Delgocitinib API manufacturers, exporters & distributors?

Delgocitinib manufacturers, exporters & distributors 1

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API | Excipient name

Delgocitinib

Synonyms

1263774-59-9, Jte-052, Jte-052a, Corectim, Leo 124249a, Leo 124249

Cas Number

1263774-59-9

Unique Ingredient Identifier (UNII)

9L0Q8KK220

About Delgocitinib

Delgocitinib is under investigation in clinical trial NCT03683719 (Phase 2b Dose-ranging Trial to Evaluate Delgocitinib Cream 1, 3, 8, and 20 Mg/g Compared to Delgocitinib Cream Vehicle Over a 16-week Treatment Period in Adult Subjects With Chronic Hand Eczema).

Delgocitinib Manufacturers

A Delgocitinib manufacturer is defined as any person or entity involved in the manufacture, preparation, processing, compounding or propagation of Delgocitinib, including repackagers and relabelers. The FDA regulates Delgocitinib manufacturers to ensure that their products comply with relevant laws and regulations and are safe and effective to use. Delgocitinib API Manufacturers are required to adhere to Good Manufacturing Practices (GMP) to ensure that their products are consistently manufactured to meet established quality criteria.

click here to find a list of Delgocitinib manufacturers with USDMF, JDMF, KDMF, CEP, GMP, and COA related information on PhamaCompass.

Delgocitinib Suppliers

A Delgocitinib supplier is an individual or a company that provides Delgocitinib active pharmaceutical ingredient (API) or Delgocitinib finished formulations upon request. The Delgocitinib suppliers may include Delgocitinib API manufacturers, exporters, distributors and traders.

click here to find a list of Delgocitinib suppliers with USDMF, JDMF, KDMF, CEP, GMP, and COA related information on PharmaCompass.

Delgocitinib GMP

Delgocitinib Active pharmaceutical ingredient (API) is produced in GMP-certified manufacturing facility.

GMP stands for Good Manufacturing Practices, which is a system used in the pharmaceutical industry to make sure that goods are regularly produced and monitored in accordance with quality standards. The FDA’s current Good Manufacturing Practices requirements are referred to as cGMP or current GMP which indicates that the company follows the most recent GMP specifications. The World Health Organization (WHO) has its own set of GMP guidelines, called the WHO GMP. Different countries can also set their own guidelines for GMP like China (Chinese GMP) or the EU (EU GMP).

PharmaCompass offers a list of Delgocitinib GMP manufacturers, exporters & distributors, which can be sorted by USDMF, JDMF, KDMF, CEP (COS), WC, and more, enabling you to easily find the right Delgocitinib GMP manufacturer or Delgocitinib GMP API supplier for your needs.

Delgocitinib CoA

A Delgocitinib CoA (Certificate of Analysis) is a formal document that attests to Delgocitinib's compliance with Delgocitinib specifications and serves as a tool for batch-level quality control.

Delgocitinib CoA mostly includes findings from lab analyses of a specific batch. For each Delgocitinib CoA document that a company creates, the USFDA specifies specific requirements, such as supplier information, material identification, transportation data, evidence of conformity and signature data.

Delgocitinib may be tested according to a variety of international standards, such as European Pharmacopoeia (Delgocitinib EP), Delgocitinib JP (Japanese Pharmacopeia) and the US Pharmacopoeia (Delgocitinib USP).

Inform the supplier about your product requirements, specifying if you need a product with particular monograph like EP (Ph. Eur.), USP, JP, BP, or any other quality. In addition, clarify whether you need hydrochloride (HCl), anhydricum, base, micronisatum or a specific level of purity. To find reputable suppliers, utilize the filters and select those certified by GMP, FDA, or any other certification as per your requirement.
For your convenience, we have listed synonyms and CAS numbers to help you find the best supplier. The use of synonyms and CAS numbers can be helpful in identifying potential suppliers, but it is crucial to note that they might not always indicate the exact same product. It is important to confirm the product details with the supplier before making a purchase to ensure that it meets your requirements.
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