Lanoracopan

CAS 2797066-85-2

MFC27H32N2O4 MW448.6 g/mol

4-[(2S,4S)-4-(cyclopropylmethoxy)-1-[(5-methoxy-7-methyl-1H-indol-4-yl)methyl]piperidin-2-yl]benzoic acid

Benzoic acid, 4-[(2S,4S)-4-(cyclopropylmethoxy)-1-[(5-methoxy-7-methyl-1H-indol-4-yl)methyl]-2-piperidinyl]-

4-{(2S,4S)-4-(cyclopropylmethoxy)-1-[(5-methoxy-7-methyl-1H-indol-4-yl)methyl]piperidin-2-yl}benzoic acid
complement factor B inhibitor, MY 008211A, Factor B-IN-5, Y5UN7AE8SF

Lanoracopan (also known by its developmental code MY008211A or Factor B-IN-5) is an investigational small-molecule drug that acts as a potent complement factor B (CFB) inhibitor. It is designed to target and regulate the alternative pathway of the complement system, which is a crucial part of the body’s innate immune defense

Clinical Development & Indications

Originally developed by Shanghai Meiyue Biotech Development Co. Ltd., the drug has transitioned from early discovery into active clinical trials. It is primarily being evaluated for:

1. Paroxysmal Nocturnal Hemoglobinuria (PNH): Lanoracopan (as MY008211A tablets) is currently undergoing Phase 2 and Phase 2/3 clinical trials. These studies assess its long-term safety, tolerability, and efficacy in patients suffering from PNH who experience active hemolysis (the premature destruction of red blood cells).
2. Renal Impairment Studies: Clinical research is also actively evaluating the drug’s safety profile and pharmacokinetics in individuals with varying degrees of kidney function.

Current Status

Lanoracopan is recognized under the World Health Organization’s proposed International Nonproprietary Names (INN) registry. It is not yet approved for public use or commercial medical prescriptions by global regulatory bodies. Currently, it is primarily available to the scientific community as a reference standard for laboratory research use only

SYN

https://patentscope.wipo.int/search/en/detail.jsf?docId=WO2023020566&_cid=P21-MQD5YH-25997-1

Example 4: 

[0727]4-((2S,4S)-4-(cyclopropylmethoxy)-1-((5-methoxy-7-methyl-1H-indol-4-yl)methyl)piperidin-2-yl)benzoic acid (compound 4) 

[0728]

4-((2S,4S)-4-(cyclopropylmethoxy)-1-((5-methoxy-7-methyl-1H-indol-4-yl)methyl)piperidin-2-yl)benzoic acid

[0755]The mixture (130 mg) of the above-mentioned tert-butyl 4-(((2S,4S)-4-(cyclopropylmethoxy)-2-(4-(((cyclopropylmethoxy)carbonyl)phenyl)piperidin-1-yl)methyl)-5-methoxy-7-methyl-1H-indole-1-carboxylic acid (tert-butyl ester) and 4-(((2S,4S)-4-(cyclopropylmethoxy)-2-(4-(methoxycarbonyl)phenyl)piperidin-1-yl)methyl)-5-methoxy-7-methyl-1H-indole-1-carboxylic acid (tert-butyl ester) (4c-2) was dissolved in 10 mL of methanol, and solid potassium carbonate (149 mg, 1.08 mmol) was added. The mixture was heated to 85 °C and refluxed for 3 h. The reaction solution was cooled to room temperature and concentrated under reduced pressure to obtain the crude product. The crude product was dissolved in a mixed solvent of 10 mL THF, 5 mL methanol, and 2 mL water. Lithium hydroxide monohydrate (181 mg, 4.3 mmol) was added, and the mixture was stirred at room temperature for 16 h. The reaction system was concentrated under reduced pressure, and the crude product was subjected to Pre-HPLC (instrument and preparative column: Glison GX-281 preparative HPLC system; Sunfire C18 column, 5 μm, inner diameter × length = 30 mm × 150 mm). Preparation method: The crude product was dissolved in methanol and dimethyl sulfoxide, and filtered through a 0.45 μm filter membrane to prepare the sample solution. Mobile phase system: acetonitrile/aqueous solution containing 5 mmol/L ammonium acetate. Gradient elution method: Acetonitrile was used to elute 60% of the solution with a 5% gradient (elution time 15 min), and the solution was lyophilized to obtain 4-((2S,4S)-4-(cyclopropylmethoxy)-1-((5-methoxy-7-methyl-1H-indol-4-yl)methyl)piperidin-2-yl)benzoic acid (compound 4) (5 mg). 

[0756]

¹H NMR(400MHz,CD ₃OD)δ8.10(d,2H),7.60(d,2H),7.28(d,1H),6.73(s,1H),6.32(s,1H),4.70–4.40(m,1H),4.32–4.14(m,1H),4.09–3.90(m,1H),3.88–3.79(m,1H),3.75(s, 3H),3.42–3.34(m,2H),3.30–3.14(m,2H),2.49(s,3H),2.26–2.10(m,2H),2.06–1.90(m,2H),1.19–1.04(m,1H),0.64–0.50(m,2H),0.31–0.22(m,2H).

[0757]

LCMS m/z＝449.2[M+1] ⁺

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PAT

• Benzo nitrogen-containing heteroaromatic ring derivative and use thereof in medicinePublication Number: WO-2023020566-A1Priority Date: 2021-08-18
• Benzo nitrogen-containing heteroaromatic ring derivative and use thereof in medicinePublication Number: US-2024383917-A1Priority Date: 2021-08-18
• A benzazaaromatic ring derivative and its application in medicinePublication Number: CN-118043314-APriority Date: 2021-08-18
• Benzo nitrogen-containing heteroaromatic ring derivative and use thereof in medicinePublication Number: EP-4389742-A1Priority Date: 2021-08-18
• Complement factor b inhibitor, and pharmaceutical composition thereof, preparation method therefor and use thereofPublication Number: EP-4194451-A1Priority Date: 2020-08-07
• Complement factor b inhibitor, and pharmaceutical composition thereof, preparation method therefor and use thereofPublication Number: EP-4282486-A2Priority Date: 2020-08-07
• Complement factor b inhibitor, and pharmaceutical composition, preparation method and use thereofPublication Number: US-2023286947-A1Priority Date: 2020-08-07

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