Rizavasertib

 

Rizavasertib

CAS 552325-16-3

MF C24H23N5O MW397.5 g/mol

(2S)-1-(1H-indol-3-yl)-3-[[5-(3-methyl-2H-indazol-5-yl)-3-pyridinyl]oxy]propan-2-amine

(2S)-1-(1H-indol-3-yl)-3-{[5-(3-methyl-1H-indazol-5-yl)pyridin-3-yl]oxy}propan-2-amine
serine/threonine kinase inhibitor, A-443654, A 443654, A443654, Q4UG565ZYH

Rizavasertib was a drug candidate originally developed by Abbott (now AbbVie).^[1][2][3][4] It is a pan akt Inhibitor.^[5] It is now used as an akt inhibitor tool compound.^[6]

Rizavasertib (also known by its developmental code A-443654) is a potent, small-molecule pan-Akt (protein kinase B) inhibitor originally developed by Abbott Laboratories (now AbbVie). It acts as a highly effective research tool compound used to investigate cellular signaling pathways, particularly in oncology and tumor cell biology

• Mechanism of Action: It is an ATP-competitive inhibitor that targets all three Akt isoforms (Akt1, Akt2, and Akt3) with equal intracellular potency, showing an inhibition constant (\(\text{K}_{i}\)) of 160 pM.

Key Biological & Research Effects

• Pathway Modulation: It induces a rapid, paradoxical phosphorylation of Akt at the Ser-473 residue, occurring independently of mTORC1 inhibition.
• Mitotic Regulation: The compound interferes with normal cell division (mitotic progression) by regulating the expression of Aurora A kinase.
• Oncology Models: In preclinical testing, it has demonstrated an ability to prolong survival in animal models of intracranial glioma and shows potential therapeutic relevance against both primary and drug-resistant T-cell acute lymphoblastic leukemia (T-ALL).

Current Status

Rizavasertib's highest global development status remains Preclinical. It is not approved for human use or clinical medical treatment and is sold exclusively by chemical suppliers like MedChemExpress as an analytical reference standard or reagent for qualitative, quantitative, and methodological research (such as HPLC, GC, and mass spectrometry).

PAT

US20030199511 and literature Bioorganic & Medicinal Chemistry 2006, 14, 6832–6846, a method for preparing A-443654 is disclosed, 

PAT

WO-03051366

https://patentscope.wipo.int/search/en/detail.jsf?docId=WO2003051366&_cid=P11-MTGMSN-41566-1

PAT

https://patentscope.wipo.int/search/en/detail.jsf?docId=US40155124&_cid=P11-MTGN0W-48129-1

SIMILAR

EXAMPLE 191

(1R)-1-(1H-Indol-3-ylmethyl)-2-[5-(3-methyl-1H-indazol-5-yl)-pyridin-3-yloxy]-ethylamine

MS (ESI) m/e 398 (M+H)+; 1H NMR (300 MHz, DMSO-D6) δ ppm 2.55 (s, 3 H) 3.16 (m, 2 H) 3.86 (d, J=1.70 Hz, 1 H) 4.19 (dd, J=10.51, 6.10 Hz, 1 H) 4.36 (dd, J=10.85, 3.39 Hz, 1 H) 7.01 (t, J=7.46 Hz, 1 H) 7.10 (t, J=6.95 Hz, 1 H) 7.30 (d, J=2.37 Hz, 1 H) 7.38 (d, J=8.14 Hz, 1 H) 7.65 (m, 5 H) 8.07 (s, 1 H) 8.16 (s, 2 H) 8.33 (d, J=2.71 Hz, 1 H) 8.63 (d, J=1.70 Hz, 1 H) 11.04 (bs, 1 H); Anal. Calcd for C24H23N5O.2.9 TFA: C, 49.16; H, 3.59; N, 9.62. Found: C, 49.36; H, 3.66; N, 9.78.

PAT

CN104610229

https://patentscope.wipo.int/search/en/detail.jsf?docId=CN133679262&_cid=P11-MTGNFX-58461-1

Example 4: Preparation of Compound 6

Compound 5 (104 g, 178.9 mmol) and methanol (620 ml, 6V) were added to a 1 L three-necked flask. A 4M HCl/ethyl acetate (130 ml) solution was added dropwise at a temperature below 25 °C. The reaction was allowed to proceed overnight. The reaction was monitored by TLC until the starting material was completely reacted. The mixture was concentrated and drained to dryness using an oil pump to obtain 104 g of crude product. Water (900 ml) and ethyl acetate (1350 ml) were added, and the mixture was stirred until the system was clear. The mixture was allowed to stand, and the organic layer was separated. The aqueous phase was extracted once again with ethyl acetate (500 ml). The organic phases were combined, and water (180 ml) was added. Most of the ethyl acetate was concentrated until solid began to precipitate. The mixture was cooled in an ice bath, stirred, and allowed to crystallize for 30 min. The mixture was filtered, and the filter cake was dried to obtain a white solid (57.9 g, yield 86%, purity 98.3%).

1H NMR(CD 3 OD,500MHz):δppm 8.45(s,1H),8.25(brs,1H),7.98(s,1H),7.61(m,4H),7.37(s,1H),7.16(s,1H),7.10(m,1H),7.00(m,1H),4.18(m,1H),4.03(m,1H),3.56(m,1H),3.10(m,1H),3.00(m,1H),2.62(s,3H)；ESI/MS:m/z＝398(M+H)+.

Pat

• Kinase inhibitorsPublication Number:US-6831175-B2Priority Date:2001-12-13Grant Date:2004-12-14
• 3- (Phenyl-alkoxy) -5- (phenyl) -pyridine derivatives and related compounds as kinase inhibitors for cancer treatmentPublication Number:JP-2005516927-APriority Date:2001-12-13
• Methods of treating muscular wasting diseases using NF-KB activation inhibitorsPublication Number:US-9173920-B2Priority Date:2006-03-15Grant Date:2015-11-03
• Kinase inhibitorsPublication Number:US-2003187026-A1Priority Date:2001-12-13
• 3-(phenyl-alkoxy)-5-(phenyl)-pyridine derivatives and related compounds as kinase inhibitors for the treatment of cancerPublication Number:CA-2470214-A1Priority Date:2001-12-13
• Kinase inhibitorsPublication Number:US-2003199511-A1Priority Date:2001-12-13
• 3-(phenyl-alkoxy)-5-(phenyl)-pyridine derivatives and related compounds as kinase inhibitors for the treatment of cancerPublication Number:WO-03051366-A2Priority Date:2001-12-13

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References

1.  "Research programme: protein kinase inhibitors - AbbVie". AdisInsight. Springer Nature Switzerland AG.
2.  Luo Y, Shoemaker AR, Liu X, Woods KW, Thomas SA, de Jong R, et al. (June 2005). "Potent and selective inhibitors of Akt kinases slow the progress of tumors in vivo". Molecular Cancer Therapeutics. 4 (6): 977–986. doi:10.1158/1535-7163.MCT-05-0005. PMID 15956255.
3.  Gandelman M, Dansithong W, Kales SC, Paul S, Maag G, Aoyama E, et al. (October 2021). "The AKT modulator A-443654 reduces α-synuclein expression and normalizes ER stress and autophagy". The Journal of Biological Chemistry. 297 (4) 101191. doi:10.1016/j.jbc.2021.101191. PMC 8482485. PMID 34520759.
4.  Ming J, Jin S, Liu Z, Yang K, Shi M, Niu Y (October 2025). "Imidacloprid contributes to bladder cancer progression: preliminary evidence based on network toxicology, machine learning and molecular docking". BMC Pharmacology & Toxicology. 26 (1) 180. doi:10.1186/s40360-025-01016-9. PMC 12577002. PMID 41168844.
5.  Crowell JA, Steele VE, Fay JR (August 2007). "Targeting the AKT protein kinase for cancer chemoprevention". Molecular Cancer Therapeutics. 6 (8): 2139–2148. doi:10.1158/1535-7163.MCT-07-0120. PMID 17699713.
6.  Garcia-Echeverria C, Sellers WR (September 2008). "Drug discovery approaches targeting the PI3K/Akt pathway in cancer". Oncogene. 27 (41): 5511–5526. doi:10.1038/onc.2008.246. PMID 18794885.

Clinical data
Other names	A-443654
Identifiers
IUPAC name
CAS Number	552325-16-3
PubChem CID	10172943
IUPHAR/BPS	8204
DrugBank	DB08073
ChemSpider	8348448
UNII	Q4UG565ZYH
ChEBI	CHEBI:91351
ChEMBL	ChEMBL379300
PDB ligand	L20 (PDBe, RCSB PDB)
CompTox Dashboard (EPA)	DTXSID20436347
Chemical and physical data
Formula	C24H23N5O
Molar mass	397.482 g·mol−1
3D model (JSmol)	Interactive image
SMILES
InChI

/////////rizavasertib, anax labs, serine/threonine kinase inhibitor, A-443654, A 443654, A443654, Q4UG565ZYH

#rizavasertib, #anax labs, #serine/threonine kinase inhibitor, #A-443654, #A 443654, #A443654, #Q4UG565ZYH

Rusfertide

 

Rusfertide

MF
C₁₁₄H₁₈₁N₂₇O₂₈S₂ MW 2442.0 g/mol

isovaleryl-Asp-Thr-His-Phe-Pro-Cys(1)-Ile-Lys(2)-Phe-Glu-Pro-Arg-Ser-Lys-Gly-Cys(1)-Lys-NH2.palmitoyl-Glu(2)-OH

(2S)-5-[4-[(3S,6S,9S,12S,15R,20R,26S,29S,32S,35S)-26-(4-aminobutyl)-6-benzyl-12-[(2S)-butan-2-yl]-32-(3-carbamimidamidopropyl)-3-(2-carboxyethyl)-15-[[(2S)-1-[(2S)-2-[[(2S)-2-[[(2S,3R)-2-[[(2S)-3-carboxy-2-(3-methylbutanoylamino)propanoyl]amino]-3-hydroxybutanoyl]amino]-3-(1H-imidazol-4-yl)propanoyl]amino]-3-phenylpropanoyl]pyrrolidine-2-carbonyl]amino]-20-[[(2S)-1,6-diamino-1-oxohexan-2-yl]carbamoyl]-29-(hydroxymethyl)-2,5,8,11,14,22,25,28,31,34-decaoxo-17,18-dithia-1,4,7,10,13,21,24,27,30,33-decazabicyclo[33.3.0]octatriacontan-9-yl]butylamino]-2-(hexadecanoylamino)-5-oxopentanoic acid

{Asp(N-(3-methyl-1-oxobutyl))}-Thr-His-Phe-Pro-Cys-Ile-{Lys(γGlu-C16 acid)}-Phe-Glu-Pro-Arg-Ser-Lys-Gly-Cys-Lys-NH2 (disulfide bridge: Cys6-Cys16)

Mimrylo, APPROVALS 2026, FDA 2026, XM71MYX0IQ, PTG-300FB, PTG-300, TAK 121,

To treat erythrocytosis in adults with polycythemia vera

Rusfertide is a peptide mimetic of natural hepcidin, which targets and degrades ferroportin, reduces serum iron and transferrin-saturation, and thus regulates the production of red blood cells. Rusfertide ameliorates the polycythemia vera, β-thalassemia and hereditary hemochromatosis.

Rusfertide is an injectable peptide mimetic of hepcidin (hepcidin antimicrobial peptide; HAMP; putative liver tumor regressor; PLTR; liver-expressed antimicrobial peptide 1; LEAP-1) with potential use in the treatment of iron deficiency anemia and iron overload secondary to hematologic disorders. Upon administration, rusfertide mimics endogenous hepcidin, a protein primarily produced in hepatocytes, and increases hepcidin levels. As hepcidin plays a key role in the homeostasis of systemic iron, rusfertide may serve to normalize iron levels. Low levels of endogenous hepcidin are associated with iron overload secondary to excessive absorption of iron as seen in beta thalassemia and paradoxically with iron deficiency anemia.

Rusfertide, sold under the brand name Mimrylo, is a medication developed by Protagonist Therapeutics in partnership with Takeda for the treatment of polycythemia vera (PV).^[1][2][3]

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References

Clinical data
Trade names	Mimrylo
Other names	PTG-300; TAK-121
Identifiers
CAS Number	1628323-80-7
PubChem CID	155884410
DrugBank	DB17724
ChemSpider	129955617
UNII	XM71MYX0IQ
KEGG	D12064
ChEMBL	ChEMBL4650507
Chemical and physical data
Formula	C114H181N27O28S2
Molar mass	2441.98 g·mol−1
3D model (JSmol)	Interactive image
SMILES
InChI

References

1.  "Rusfertide - Protagonist Therapeutics". AdisInsight. Springer Nature Switzerland AG.
2.  Kremyanskaya M, Ginzburg YZ, Hoffman R (March 2026). "Modulators of the hepcidin pathway in polycythemia vera and myelofibrosis". Blood. 147 (12): 1278–1288. doi:10.1182/blood.2025028643. PMID 41100735.
3.  "Protagonist and Takeda Announce ASCO Plenary Presentation Highlighting Full 32-Week Results from Phase 3 VERIFY Study of Rusfertide, Showing Reductions in Phlebotomy, Improved Hematocrit Control in Polycythemia Vera". Takeda.

//////rusfertide, anax labs, Mimrylo, APPROVALS 2026, FDA 2026, XM71MYX0IQ, PTG-300FB, PTG 300, TAK 121,

#rusfertide, #anax labs, #Mimrylo, #APPROVALS 2026, #FDA 2026, #XM71MYX0IQ, #PTG-300FB, #PTG-300, #TAK 121, 

Brepocitinib

 

Brepocitinib

CAS 1883299-62-4

MF C₁₈H₂₁F₂N₇O MW389.4 g/mol

8/27/2026, APPROVALS 2026, FDA 2026, Lisraya, PF 06700841, 3X8387Q25N, PF-06700841

[(1S)-2,2-difluorocyclopropyl]-[(1R,5S)-3-[2-[(1-methylpyrazol-4-yl)amino]pyrimidin-4-yl]-3,8-diazabicyclo[3.2.1]octan-8-yl]methanone

• [(1S)-2,2-difluorocyclopropyl]-[(1S,5R)-3-[2-[(1-methylpyrazol-4-yl)amino]pyrimidin-4-yl]-3,8-diazabicyclo[3.2.1]octan-8-yl]methanone
• Methanone, ((1S)-2,2-difluorocyclopropyl)(3-(2-((1-methyl-1H-pyrazol-4-yl)amino)-4-pyrimidinyl)-3,8-diazabicyclo(3.2.1)oct-8-yl)-
• ((1S)-2,2-difluorocyclopropyl)-((1S,5R)-3-(2-((1-methylpyrazol-4-yl)amino)pyrimidin-4-yl)-3,8-diazabicyclo(3.2.1)octan-8-yl)methanone

To treat dermatomyositis in adults

Brepocitinib (brand name Lisraya) is an oral, once-daily dual TYK2/JAK1 inhibitor approved by the FDA for treating dermatomyositis in adults.

Developed by Roivant (via its subsidiary Priovant), it is the first oral targeted therapy indicated to manage this rare, debilitating autoimmune condition. Brepocitinib, sold under the brand name Lisraya, is a drug which acts as a dual inhibitor of JAK1 and TYK2, and was developed for the treatment of plaque psoriasis.^[1][2][3][4] It is used for the treatment of dermatomyositis.

Brepocitinib is an orally available, selective inhibitor of non-receptor tyrosine-protein kinase TYK2 (tyrosine kinase 2) and tyrosine-protein kinase JAK1 (Janus kinase 1; JAK1) with potential immunomodulatory and anti-inflammatory activities. Upon oral administration, brepocitinib selectively binds to and inhibits the activation of TYK2 and JAK1, thereby disrupting TYK2 and JAK-1-dependent cytokine signaling. This may reduce inflammatory responses and prevent inflammation-induced damage caused by certain immunological diseases. TYK2 and JAK-1 are members of the Janus kinase family of non-receptor tyrosine kinases and are involved in signaling pathways affecting hematopoiesis, immunity and inflammation.

SYN

Dual Inhibition of TYK2 and JAK1 for the Treatment of Autoimmune Diseases: Discovery of ((S)-2,2-Difluorocyclopropyl)((1R,5S)-3-(2-((1-methyl-1H-pyrazol-4-yl)amino)pyrimidin-4-yl)-3,8-diazabicyclo[3.2.1]octan-8-yl)methanone (PF-06700841)

By: Fensome, Andrew ; et al

Journal of Medicinal Chemistry (2018), 61(19), 8597-8612

SYN

Preparation of aminopyrimidinyl derivatives as inhibitors of JAK kinases useful in therapy of diseases

Assignee: Pfizer Inc.

Inventors: Fensome, Andrew; et al

World Intellectual Property Organization

Patent#WO2016027195 A1

https://patentscope.wipo.int/search/en/detail.jsf?docId=WO2016027195&_cid=P11-MTCC5U-40903-1

SYN

https://www.sciencedirect.com/science/article/abs/pii/S0223523423008152

SYN

compound 23 [PMID: 30113844]

PAT

US9663526,

https://patentscope.wipo.int/search/en/detail.jsf?docId=US159751917&_cid=P11-MTCCDC-53135-1

Examples 7 and 8

[(1S)-2,2-difluorocyclopropyl][(1R,5S)-3-{2-[(1-methyl-1H-pyrazol-4-yl)amino]pyrimidin-4-yl}-3,8-diazabicyclo[3.2.1]oct-8-yl]methanone and [(1R)-2,2-difluorocyclopropyl][(1R,5S)-3-{2-[(1-methyl-1H-pyrazol-4-yl)amino]pyrimidin-4-yl}-3,8-diazabicyclo[3.2.1]oct-8-yl]methanone

To a solution of (S)-2,2-difluorocyclopropane-1-carboxylic acid (Preparation 68, 318 mg, 2.61 mmol) in DCM (20 mL) was added 4-((1R,5S)-3,8-diazabicyclo[3.2.1]octan-3-yl)-N-(1-methyl-1H-pyrazol-4-yl)pyrimidin-2-amine hydrochloride (Preparation 19, 700 mg, 2.17 mmol), HATU (1.02 g, 2.61 mmol and DIPEA (0.76 mL, 4.34 mmol) and the reaction was stirred at room temperature for 18 hours. The reaction was diluted with DCM and saturated aqueous ammonium chloride solution. The organic layer was separated, washed with further ammonium chloride solution and concentrated in vacuo. The residue was purified using silica gel column chromatography eluting with 0-12% MeOH and 1% NH 4OH in DCM. The residue was dissolved in DCM and further washed with saturated aqueous ammonium chloride solution three times. The organic layer was collected, concentrated in vacuo and dried to afford the title compound (500 mg, 60%).

The title compound and its enantiomer may also be prepared according to the same method using racemic 2,2-difluorocyclopropane-1-carboxylic acid with additional chiral separation of the enantiomers after purification using the method below to afford:

Peak 1: Example 7

[(1S)-2,2-difluorocyclopropyl][(1R,5S)-3-{2-[(1-methyl-1H-pyrazol-4-yl)amino]pyrimidin-4-yl}-3,8-diazabicyclo[3.2.1]oct-8-yl]methanone

1H NMR (400 MHz, DMSO-d 6): δ ppm 1.58-2.06 (m, 6H), 2.82-3.27 (m, 3H), 3.80 (s, 3H), 4.14 (br s, 2H), 4.55-4.74 (m, 2H), 6.07-6.19 (m, 1H), 7.44 (s, 1H), 7.74 (brs, 1H), 7.93 (d, 1H), 8.90 (brs, 1H). MS m/z 390 [M+H]; [α] D 2050.1 (c 1.27, EtOH)

PAT

• New compounds for the inhibition of angiogenesis and use of thereofPublication Number:AU-2005223356-A1Priority Date:2004-03-24
• Compositions and methods of use for modified release minoxidilPublication Number:US-2025325546-A1
• Aminopyrimidinyl compoundsPublication Number:US-10980815-B2Priority Date:2014-08-21Grant Date:2021-04-20
• Aminopyrimidinyl compounds as JAK inhibitorsPublication Number:MD-4800-C1Priority Date:2014-08-21
• Aminopyrimidinyl compoundsPublication Number:US-2020330477-A1Priority Date:2014-08-21
• Aminopyrimidinyl compoundsPublication Number:US-11197867-B2Priority Date:2014-08-21Grant Date:2021-12-14
• Aminopyrimidinyl compoundsPublication Number:TW-201609706-APriority Date:2014-08-21

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References

References

1.  Fensome A, Ambler CM, Arnold E, Banker ME, Brown MF, Chrencik J, et al. (October 2018). "Dual Inhibition of TYK2 and JAK1 for the Treatment of Autoimmune Diseases: Discovery of (( S)-2,2-Difluorocyclopropyl)((1 R,5 S)-3-(2-((1-methyl-1 H-pyrazol-4-yl)amino)pyrimidin-4-yl)-3,8-diazabicyclo[3.2.1]octan-8-yl)methanone (PF-06700841)". Journal of Medicinal Chemistry. 61 (19): 8597–8612. doi:10.1021/acs.jmedchem.8b00917. PMID 30113844.
2.  Forman SB, Pariser DM, Poulin Y, Vincent MS, Gilbert SA, Kieras EM, et al. (December 2020). "TYK2/JAK1 Inhibitor PF-06700841 in Patients with Plaque Psoriasis: Phase IIa, Randomized, Double-Blind, Placebo-Controlled Trial". The Journal of Investigative Dermatology. 140 (12): 2359–2370.e5. doi:10.1016/j.jid.2020.03.962. PMID 32311398.
3.  Martin G (February 2023). "Novel Therapies in Plaque Psoriasis: A Review of Tyrosine Kinase 2 Inhibitors". Dermatology and Therapy. 13 (2): 417–435. doi:10.1007/s13555-022-00878-9. PMC 9884727. PMID 36592300.
4.  Caso F, Costa L, Triggianese P, Maione F, Bertolini N, Vastarella M, et al. (May 2023). "Recent developments for new investigational JAK inhibitors in psoriatic arthritis". Expert Opinion on Investigational Drugs. 32 (5): 361–371. doi:10.1080/13543784.2023.2207737. PMID 37096862.

Clinical data
Trade names	Lisraya
Other names	PF-06700841
Identifiers
IUPAC name
CAS Number	1883299-62-4
PubChem CID	118878093
DrugBank	DB15003
ChemSpider	72380129
UNII	3X8387Q25N
ChEMBL	ChEMBL4297477
Chemical and physical data
Formula	C18H21F2N7O
Molar mass	389.411 g·mol−1
3D model (JSmol)	Interactive image
SMILES
InChI

///////////brepocitinib, anax labs, APPROVALS 2026, FDA 2026, Lisraya, PF 06700841, 3X8387Q25N, PF-06700841, dermatomyositis

#brepocitinib, #anax labs, #APPROVALS 2026, #FDA 2026, #Lisraya, #PF 06700841, #3X8387Q25N, #PF-06700841, #dermatomyositis

Rezuforimod

 

Rezuforimod

CAS 1431754-15-2

MF C15H20BrN3O4, MW386.24 g/mol

((4-Bromophenyl)carbamoyl)-L-leucylglycine

2-[[(2S)-2-[(4-bromophenyl)carbamoylamino]-4-methylpentanoyl]amino]acetic acid

N-[(4-bromophenyl)carbamoyl]-L-leucylglycine
N-formyl peptide receptor 1 and 2 agonist, antiinflammatory, AGN-232411, AG-80308, AGN 232411, AG 80308, 54P16AUY6D

Rezuforimod is an experimental drug that acts as a potent and selective agonist of formyl peptide receptor 2 with an EC₅₀ of 0.88 nM, which inhibits neutrophil adhesion and has antiinflammatory effects.^[1][2]

Rezuforimod (also known by development codes AGN-232411 and AG-80308) is an experimental, first-in-class small molecule drug primarily being developed as a topical ophthalmic solution to treat dry eye disease (DED). It targets inflammation, which is a major underlying driver of dry eye symptoms and ocular surface damage.

---

👁️ Mechanism of Action

Rezuforimod operates through a targeted anti-inflammatory pathway:

• FPR2 Agonism: It acts as a highly potent and selective agonist of Formyl Peptide Receptor 2 (FPR2/ALX), binding with an EC₅₀ of 0.88 nM.
• Neutrophil Inhibition: Activating this receptor successfully inhibits neutrophil adhesion and migration to the ocular surface.
• Inflammation Resolution: By mimicking natural pro-resolving leagues, it shuts down chronic inflammatory cascades on the corneal surface rather than just suppressing the immune system globally.

🔬 Clinical Trial Findings & Efficacy

In clinical assessments, Rezuforimod has shown excellent potential as a localized therapy:

• Dosing: It is formulated as an eye drop administered twice daily (BID).
• Objective Improvement: Over a 3-month trial period, it significantly reduced corneal and conjunctival staining scores (an objective measure of tissue damage on the surface of the eye). The most pronounced improvements were recorded at Day 43 and Day 84.
• Subjective Relief: Patients reported a notable reduction in daily ocular discomfort and an improved Ocular Surface Disease Index (OSDI) score.
• Safety Profile: The drug has demonstrated a favorable safety profile with no serious drug-related adverse events, and no abnormal shifts in vital signs or systemic blood chemistry.

A Study of AG-80308 in Dry Eye PatientsCTID:NCT05372107, Phase: Phase 1

Status:Completed, Date:2022-11-29

SYN

• The formyl peptide receptors FPR1 and FPR2 as targets for inflammatory disorders: recent advances in the development of small-molecule agonistsPublication Name:European Journal of Medicinal ChemistryPublication Date:2024-02-05PMID:38199163DOI:10.1016/j.ejmech.2023.115989
• Synthesis and evaluation of novel cyclopentane urea FPR2 agonists and their potential application in the treatment of cardiovascular inflammationPublication Name:European Journal of Medicinal ChemistryPublication Date:2021-03-15PMID:33548634DOI:10.1016/j.ejmech.2021.113194
• Recent advances in the design and development of formyl peptide receptor 2 (FPR2/ALX) agonists as pro-resolving agents with diverse therapeutic potentialPublication Name:European Journal of Medicinal ChemistryPublication Date:2021-03-05PMID:33486199DOI:10.1016/j.ejmech.2021.113167

PAT

US10208071, Compound 8

https://patentscope.wipo.int/search/en/detail.jsf?docId=US205825234&_cid=P10-MT81MF-62360-1

PAT

WO2013062947 

https://patentscope.wipo.int/search/en/detail.jsf?docId=WO2013062947&_cid=P10-MT81PJ-63770-1

PAT

• Amide derivatives of N-urea substituted amino acids as formyl peptide receptor like-1 (FPRL-1) receptor modulatorsPublication Number:US-10993931-B2Priority Date:2011-10-26Grant Date:2021-05-04
• Amide derivatives of n-urea substituted amino acids as formyl peptide receptor like-1 (fprl-1) receptor modulatorsPublication Number:WO-2013062947-A1Priority Date:2011-10-26
• Substituted N-urea amino acid amide derivatives as modulators of formylated peptide receptor 1 (FPRL-1) receptorPublication Number:ES-2820714-T3Priority Date:2011-10-26Grant Date:2021-04-22
• Amide derivatives of N-urea-substituted amino acids as formyl peptide receptor-like-1 (FPRL-1) receptor modulatorsPublication Number:CN-106518742-APriority Date:2011-10-26

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References

References

1.  Maciuszek M, Cacace A, Brennan E, Godson C, Chapman TM (March 2021). "Recent advances in the design and development of formyl peptide receptor 2 (FPR2/ALX) agonists as pro-resolving agents with diverse therapeutic potential". European Journal of Medicinal Chemistry. 213 113167. doi:10.1016/j.ejmech.2021.113167. PMID 33486199.
2.  Maciuszek M, Ortega-Gomez A, Maas SL, Perretti M, Merritt A, Soehnlein O, et al. (March 2021). "Synthesis and evaluation of novel cyclopentane urea FPR2 agonists and their potential application in the treatment of cardiovascular inflammation". European Journal of Medicinal Chemistry. 214 113194. doi:10.1016/j.ejmech.2021.113194. PMID 33548634.

Identifiers
IUPAC name
CAS Number	1431754-15-2
PubChem CID	71526099
UNII	54P16AUY6D
ChEMBL	ChEMBL4785302
Chemical and physical data
Formula	C15H20BrN3O4
Molar mass	386.246 g·mol−1
3D model (JSmol)	Interactive image
SMILES
InChI

////////rezuforimod, anax labs, N-formyl peptide receptor 1 and 2 agonist, antiinflammatory, AGN-232411, AG-80308, AGN 232411, AG 80308, 54P16AUY6D

#rezuforimod, #anax labs, #N-formyl peptide receptor 1 and 2 agonist, #antiinflammatory, #AGN-232411, #AG-80308, #AGN 232411, #AG 80308, #54P16AUY6D