Amsulostat

 

Amsulostat

CAS 2409963-83-1

MF C13H13FN2O2S MW280.32

2-Buten-1-amine, 3-fluoro-4-(8-quinolinylsulfonyl)-, (2Z)-

(2Z)-3-fluoro-4-(quinolin-8-ylsulfonyl)but-2-en-1-amine

(Z)-3-fluoro-4-quinolin-8-ylsulfonylbut-2-en-1-amine

(2Z)-3-fluoro-4-(quinolin-8-ylsulfonyl)but-2-en-1-amine
protein-lysine-oxidase (LOX) inhibitor, antifibrotic,  PXS 5505, LOX inhibitor PXS-5505, LOX-IN-3, pan-LOX inhibitor PXS-5505, DO94E28WYW, SNT 5505

Amsulostat is an orally available, small-molecule, irreversible inhibitor of all lysyl oxidases (LOX) family members, with potential antifibrotic activity. Upon oral administration, amsulostat targets, binds to and inhibits the activity of all enzymes in the LOX family. This prevents the post-translational oxidative deamination of lysine residues on target proteins, including collagen and elastin, and reduces the formation of deaminated lysine (allysine), the formation of inter- and intramolecular cross-linkages and may prevent remodeling of the extracellular matrix (ECM), thereby reducing fibrotic tissue formation in certain chronic fibrotic diseases. LOX is often upregulated in fibrotic tissue and plays a key role in fibrosis.

Amsulostat (formerly PXS-5505) is an orally available, investigational, pan-lysyl oxidase (pan-LOX) inhibitor designed by Syntara to treat fibrotic diseases and solid tumors. It works by preventing collagen cross-linking and remodeling of the extracellular matrix, effectively reducing fibrosis. The drug is currently in Phase 2 clinical trials for myelofibrosis, showing promise in reducing symptom burden and spleen volume, and is also being studied for myelodysplastic syndrome (MDS) and pancreatic cancer. 

Key Aspects of Amsulostat:

• Mechanism of Action: Irreversibly inhibits all LOX family members (LOX, LOXL1-4), reducing fibrotic tissue.
• Clinical Status (Myelofibrosis): Phase 2a data showed 73% of patients (who were suboptimal responders to ruxolitinib) achieved  reduction in total symptom score, with significant spleen volume reduction.
• Clinical Status (Other Cancers): Phase 2 trials (AZALOX) are evaluating its use in myelodysplastic syndrome (MDS) and chronic myelomonocytic leukemia (CMML). It is also being tested in combination with chemotherapy for pancreatic cancer to improve drug delivery to tumors.
• Regulatory Status: Has received Orphan Drug Designation for primary myelofibrosis from the FDA (USA) and EMA (Europe).
• Safety Profile: Clinical trials have reported it is well-tolerated with no treatment-related serious adverse events in early findings.

Amsulostat's ability to target the stiff, fibrotic environment surrounding tumors makes it a promising "add-on" therapy to increase the effectiveness of existing cancer treatments, including chemotherapy and immunotherapy.

An orally available, small-molecule, irreversible inhibitor of all lysyl oxidases (LOX) family members, with potential antifibrotic activity. Upon oral administration, amsulostat targets, binds to and inhibits the activity of all enzymes in the LOX family. This prevents the post-translational oxidative deamination of lysine residues on target proteins, including collagen and elastin, and reduces the formation of deaminated lysine (allysine), the formation of inter- and intramolecular cross-linkages and may prevent remodeling of the extracellular matrix (ECM), thereby reducing fibrotic tissue formation in certain chronic fibrotic diseases. LOX is often upregulated in fibrotic tissue and plays a key role in fibrosis.

SYN

US12178791,

Compound 33

syn

https://patentscope.wipo.int/search/en/detail.jsf?docId=WO2020024017&_cid=P20-MNDZVP-86742-1

(Z)-3-fluoro-4-(quinolin-8-ylsulfonyl)but-2-en-1-amine dihydrochloride (Compound 33)

[0282] White solid; m.p.150-153 °C; ¹H NMR (300 MHz, CD3OD) d ppm: 9.18 (d, J = 4.7 Hz, 1H), 8.70 (dd, J = 8.4, 2.6 Hz, 1H), 8.57 (d, J = 7.4 Hz, 1H), 8.45 (d, J = 8.5 Hz, 1H), 7.99– 7.68 (m, 2H), 5.22 (dt, J = 32.9, 7.4 Hz, 1H), 5.00 (d, J = 19.4 Hz, 2H), 3.60 (d, J = 7.7 Hz, 2H); LCMS: for C₁₃H₁₃FN₂O₂S calculated 280.1, found 281.1 [M+1]⁺.

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References

• Haloallylamine sulfone derivative inhibitors of lysyl oxidases and uses thereofPublication Number: EP-3829520-B1Priority Date: 2018-08-03Grant Date: 2024-11-27
• Haloallylamine sulfone derivative inhibitors of lysyl oxidases and uses thereofPublication Number: US-2025082593-A1Priority Date: 2018-08-03
• Haloallylamine sulfone derivative inhibitors of lysyl oxidases and uses thereofPublication Number: US-2021353571-A1Priority Date: 2018-08-03
• Lox enzyme inhibiting methods and compositionsPublication Number: EP-4138824-A1Priority Date: 2020-04-21
• Haloallylamine sulfone derivative inhibitors of lysyl oxidases and uses thereofPublication Number: WO-2020024017-A1Priority Date: 2018-08-03
• Inhibitors of haloallylamine sulfone derivatives of lysyl oxidase and uses thereofPublication Number: KR-20210045984-APriority Date: 2018-08-03
• Halide allylamine derivate inhibitor for amine oxidase and its usePublication Number: TW-202019877-APriority Date: 2018-08-03
• Haloallylamine sulfone derivative inhibitors of lysyl oxidases and uses thereofPublication Number: US-12178791-B2Priority Date: 2018-08-03Grant Date: 2024-12-31
• Bithiazol deratives as inhibitors of lysyl oxidasesPublication Number: EP-4333843-A1Priority Date: 2021-05-13
• Inhibitors of lysyl oxidasesPublication Number: US-11712437-B2Priority Date: 2021-05-13Grant Date: 2023-08-01
• Method for selecting cancer patients for whom combination therapy of retinoid with cancer therapeutic agent is effective, and combination drug of retinoid with cancer therapeutic agentPublication Number: CN-115997122-APriority Date: 2020-06-26
• Method for selecting cancer patient for which combination therapy of retinoid and cancer treatment agent will be effective, and combined drug of retinoid and cancer treatment agentPublication Number: EP-4173639-A1Priority Date: 2020-06-26
• Method for selecting cancer patients for whom combination therapy with retinoid and cancer therapeutic agent is effective, and combination medicament with retinoid and cancer therapeutic agentPublication Number: US-2023301950-A1Priority Date: 2020-06-26

//////////// #amsulostat, #ANAX LAB, #protein-lysine-oxidase (LOX) inhibitor, #antifibrotic, #PXS 5505, #LOX inhibitor PXS-5505, #LOX-IN-3, #pan-LOX inhibitor PXS-5505, #DO94E28WYW, #SNT 5505

amsulostat, ANAX LAB, protein-lysine-oxidase (LOX) inhibitor, antifibrotic,  PXS 5505, LOX inhibitor PXS-5505, LOX-IN-3, pan-LOX inhibitor PXS-5505, DO94E28WYW, SNT 5505

Andamertinib

 

Andamertinib

CAS 2254145-43-0

MF C31H36N8O3 MW568.7 g/mol

N-[4-methoxy-2-[4-(3-methoxyazetidin-1-yl)piperidin-1-yl]-5-[[6-(1-methylindazol-5-yl)pyrimidin-4-yl]amino]phenyl]prop-2-enamide

N-(4-methoxy-2-[4-(3-methoxyazetidin-1-yl)piperidin-1-yl]-5-{[6-(1-methyl-1H-indazol-5-yl)pyrimidin-4-yl]amino}phenyl)prop-2-enamide
epidermal growth factor receptor tyrosine kinase inhibitor, antineoplastic, PLB 1004, 5X3KAG7ZBW

Andamertinib (also known as PLB1004) is an investigational, orally bioavailable, and irreversible small-molecule inhibitor of the epidermal growth factor receptor (EGFR). It is primarily being developed to treat non-small cell lung cancer (NSCLC) with specific genetic mutations. 

Key Clinical & Therapeutic Features

• Target Mutations: It specifically targets EGFR exon 20 insertion (ex20ins) mutations, which are often resistant to standard first- and second-generation EGFR inhibitors.
• Broad Selectivity: Beyond ex20ins, it also shows activity against classical mutations like Del19, L858R, and the resistance mutation T790M.
• Brain Penetration: Andamertinib is designed to cross the blood-brain barrier, making it potentially effective for patients with brain metastases.
• Clinical Performance: In phase 2 studies (e.g., the KANNON study), it demonstrated a confirmed objective response rate (ORR) of 42.7% and a median progression-free survival of 6.2 months in pretreated patients. 

Regulatory Status (as of Early 2026)

• China: A New Drug Application (NDA) was accepted by the National Medical Products Administration (NMPA) in May 2025 and granted priority review for treating NSCLC with EGFR ex20ins mutations.
• Global: It remains in various stages of clinical trials globally, including studies for first-line treatment and combination therapies with other agents like vebreltinib. 

Andamertinib is an orally bioavailable, mono-anilino-pyrimidine, mutant-selective epidermal growth factor receptor (EGFR) inhibitor, with potential antineoplastic activity. Upon oral administration, andamertinib targets, binds to and irreversibly inhibits the activity of various EGFR mutations, including exon 20 insertion (Ex20ins) activating mutations, the gatekeeper mutation T790M, ExDel19, and L858R. This prevents EGFR-mediated signaling, induces cell death and inhibits tumor growth in tumor cells expressing these EGFR mutations. EGFR, a receptor tyrosine kinase mutated in many tumor cell types, plays a key role in tumor cell proliferation and tumor vascularization.

SYN

[WO2018228446A1]

SYN

https://patentscope.wipo.int/search/en/detail.jsf?docId=US290822182&_cid=P22-MNGUGQ-15704-1

ANAX LABORATORIES

WEBSITE https://www.anaxlab.com/

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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

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References

• Aminopyrimidine compound, preparation method therefor and use thereofPublication Number: US-11352352-B2Priority Date: 2017-06-13Grant Date: 2022-06-07
• Aminopyrimidine compound, preparation method therefor and use thereofPublication Number: EP-3640248-A1Priority Date: 2017-06-13
• Aminopyrimidine compound, preparation method therefor and use thereofPublication Number: US-2020087296-A1Priority Date: 2017-06-13
• Aminopyrimidine derivatives, preparation method therefor and use thereofPublication Number: EP-3640248-B1Priority Date: 2017-06-13Grant Date: 2023-08-23

//////////andamertinib, FLAX LAB, antineoplastic, PLB 1004, 5X3KAG7ZBW

#andamertinib, #FLAX LAB, #antineoplastic, #PLB 1004, #5X3KAG7ZBW

DELOCAMTEN

 

Delocamten

CAS 2417411-02-8

MFC19H21F2N3O3 MW377.4 g/mol

Pyrido[2,3-d]pyrimidine-2,4(1H,3H)-dione, 6-fluoro-7-(2-fluoro-5-methylphenyl)-5,6,7,8-tetrahydro-3-(tetrahydro-2H-pyran-4-yl)-, (6S,7S)-

(6S,7S)-6-fluoro-7-(2-fluoro-5-methylphenyl)-3-(oxan-4-yl)-5,6,7,8-tetrahydro-1H-pyrido[2,3-d]pyrimidine-2,4-dione

(6S,7S)-6-fluoro-7-(2-fluoro-5-methylphenyl)-3-(oxan-4-yl)-5,6,7,8-tetrahydropyrido[2,3-d]pyrimidine-2,4(1H,3H)-dione
cardiac myosin inhibitor, MYK-224; BMS-986435, MYK 224, BMS 986435, IE5886BN8T

Delocamten (development code MYK-224) is a small-molecule cardiac myosin inhibitor developed by Bristol Myers Squibb for hypertrophic cardiomyopathy.^[1][2][3]

Delocamten is a small molecule drug. Delocamten is under investigation in clinical trial NCT06122779 (Study to Evaluate Safety, Tolerability and Drug Levels of BMS-986435/MYK-224 in Participants With Heart Failure With Preserved Ejection Fraction (HFpEF)). Delocamten has a monoisotopic molecular weight of 377.16 Da.

SYN

• US20250282779,

Example 1-3: Preparation of (6S,7S)-6-fluoro-7-(2-fluoro-5-methylphenyl)-3-(tetrahydro-2H-pyran-4-yl)-5,6,7,8-tetrahydropyrido[2,3-d]pyrimidine-2, 4 (1H, 3H)-dione (3)

  Step 7. Synthesis of (6S,7S)-6-fluoro-7-(2-fluoro-5-methylphenyl)-3-(tetrahydro-2H-pyran-4-yl)-5,6,7,8-tetrahydropyrido[2,3-d]pyrimidine-2, 4 (1H, 3H)-dione (3). A mixture of crude 3G (1.0 g, 2.53 mmol) in CH ₃CN (15 mL) was put into a microwave reactor with stirring at 120° C. for 30 min. Subsequently, the mixture was concentrated and the residue was purified by preparative HPLC (column: C18 silica gel; mobile phase: CH3CN:H ₂O=20:80 (v v) increasing to CH3CN:H ₂O=80:20 (v v) within 40 min; detector: UV 254 nm) to give compound 3 (302 mg, 32%), as a white solid, which was identified as Form 1 polymorph (see Example 2). LC-MS (ES, m/z): 378 [M+H] ⁺; ¹H NMR (300 MHz, d-DMSO): δ 10.20 (s, 1H), 7.38-7.05 (m, 3H), 6.45 (s, 1H), 5.11-4.81 (m, 3H), 3.89 (dd, J=10.8, 3.9 Hz, 2H), 3.34-3.27 (m, 3H), 2.76-2.48 (m, 4H), 2.28 (s, 3H), 1.39-1.36 (m, 2H); ¹⁹F NMR (376 MHz, d ⁶-DMSO): δ −123.51 (t, J=86.5 Hz), −191.57 (d, J=129.34 Hz).

PAT

https://patentscope.wipo.int/search/en/detail.jsf?docId=WO2020092208&_cid=P10-MOKV4B-54959-1

Example 1-3: Preparation of (6S,7S)-6-fluoro-7-(2-fluoro-5-methylphenyl)-3- (tetrahydro-2H-pyran-4-yl)-5,6,7,8-tetrahydropyrido[2,3-d]pyrimidine-2, 4 (1H, 3H)-dione (3).

Scheme 3

[0165] Step 1. Synthesis of (R,E)-N-(2-fluoro-5-methylbenzylidene)-2-methylpropane-2-sulfinamide (3B). The reaction mixture was filtered and the filtrate was diluted with ether (150 mL). Subsequently, the resulting suspension was filtered. The filtrate was concentrated and the residue was dried in vacuo to give 3B (8.7 g, 97%) as a yellow oil. LC-MS (ES, m/z): 242 [M+H] ⁺ ; ¹ H NMR (400 MHz, d ⁶ -DMSO): d 8.87 (s, 1H), 7.76 (m, 1H), 7.29 (m, 1H), 7.03 (m, 1H), 2.37 (d, J = 1.0 Hz, 3H), 1.27 (s, 9H).

[0166] Step 2. Synthesis of ethyl (2R,3S)-3-(((R)-tert-butylsulfinyl)amino)-2-fluoro-3-(2-fluoro-5-methylphenyl)propanoate (3C). To a solution of 3B (4 g, 16.6 mmol), ethyl 2- fluoroacetate (2.6 g, 24.6 mmol), and TMEDA (4.8 mL) in anhydrous THF (40 mL) was added LiHMDS (1 M in THF, 24.6 mL, 24.6 mmol) dropwise at -78 ^o C over 30 min under an atmosphere of Ar. After stirring at -78 ^o C for 1 h, the reaction was quenched by adding 1 N aq.

HCl (50 mL), while maintaining the inner temperature of the mixture at < -20 ^o C. Subsequently, the mixture was concentrated to remove most of the organic solvent and then extracted with EtOAc (100 mL x 3). The combined organic extracts were washed with brine (100 mL) and dried over anhydrous Na2SO4. The solvent was removed and the residue was dried in vacuo to give crude 3C (6.0 g) as a yellow oil, which was used for the next step without further purification. LC-MS (ES, m/z): 348 [M+H] ⁺ .

[0167] Step 3. Synthesis of (2R,3S)-3-(((R)-tert-butylsulfinyl)amino)-2-fluoro-3-(2-fluoro-5-methylphenyl)propanoic acid (3D). To a solution of 3C (6.0 g, 17.3 mmol) in THF (40 mL) was added 1N aq. NaOH (34.6 mL, 34.6 mmol) at rt. After stirring at rt for 1 h, the reaction mixture was added ice water (50 mL). The resulting mixture was extracted with EtOAc (100 mL x 2). The aqueous layer was adjusted to pH 5 with sat. aq. citric acid, followed by extraction with EtOAc (100 mL x 3). Subsequently, the combined organic extracts were washed with brine (100 mL) and dried over anhydrous Na ₂ SO ₄ . The solvent was removed and the residue was purified by preparative HPLC (Column: LC-MS (ES, m/z): 320 [M+H] ⁺ ; ¹ H NMR (400 MHz, d ⁶ -DMSO): d 13.57 (br, 1H), 7.55 (dd, J = 7.5, 2.2 Hz, 1H), 7.23– 6.94 (m, 2H), 6.04 (d, J = 10.8 Hz, 1H), 5.37– 4.86 (m, 2H), 2.29 (s, 3H), 1.12 (s, 9H).

[0168] Step 4. Synthesis of (R)-N-((1S,2R)-2-fluoro-1-(2-fluoro-5-methylphenyl)-3-oxo-3- (2,4,6-trioxo-1-(tetrahydro-2H-pyran-4-yl)hexahydropyrimidin-5-yl)propyl)-2-methylpropane-2-sulfinamide (3E). A solution of 3D (700 mg, 2.19 mmol), 2-2 (698 mg, 3.29 mmol), and HATU (1.25 g, 3.29 mmol) in DMF (10 mL) was added DIEA (849 mg, 6.57 mmol) at 0 ^o C under an atmosphere of Ar. aq. sodium bicarbonate (30 mL) and the resulting solution was extracted with ethyl acetate (50 mL x3). The combined organic extracts were washed with brine (50 mL x 2) and dried over anhydrous Na ₂ SO ₄ . The solvent was removed and the residue was dried in vacuo to give crude 3E (1.3 g) as a white solid, which was used for the next step without further purification. LC-MS (ES, m/z): 514 [M+H] ⁺ ; ¹ H NMR (400 MHz, d ⁶ -DMSO): d 12.16 (br, 1H), 7.66– 7.45 (m, 1H), 7.23– 6.98 (m, 2H), 6.37 (m, 1H), 6.13 (d, J = 10.7 Hz, 1H), 5.22 (m, 1H), 4.79 (m, 1H), 3.94 (m, 2H), 3.35 (t, J = 11.7 Hz, 2H), 2.52– 2.39 (m, 2H), 2.29 (s, 3H), 1.49 (d, J = 12.2 Hz, 2H), 1.04 (s, 9H).

[0169] Step 5. Synthesis of (R)-N-((1S,2S)-2-fluoro-1-(2-fluoro-5-methylphenyl)-3-(2,4,6- trioxo-1-(tetrahydro-2H-pyran-4-yl)hexahydropyrimidin-5-yl)propyl)-2-methylpropane-2-sulfinamide (3F). A solution of crude 3E (1.3 g, 2.53 mmol) in AcOH (10 mL) was added NaBH3CN (398 mg, 6.33 mmol) at 0 ^o C under an atmosphere of Ar. After stirring at rt for 1 h, the reaction mixture was added ice water (20 mL) and the resulting solution was extracted with EtOAc (50 mL x 3). Next, the combined organic extracts were washed with brine (50 mL) and

dried over anhydrous Na2SO4. The solvent was removed and the residue was dried in vacuo to give crude 3F (1.3 g) as a white solid, which was used for the next step without further purification. LC-MS (ES, m/z): 500 [M+H] ⁺ ; ¹ H NMR (400 MHz, d ⁶ -DMSO): d 11.31 (d, J = 28.1 Hz, 1H), 7.41 (d, J = 7.4 Hz, 1H), 7.27– 6.84 (m, 2H), 6.11– 5.78 (m, 2H), 5.08– 4.43 (m, 3H), 3.87 (m, 3H), 2.29 (s, 6H), 1.99 (s, 1H), 1.53– 1.28 (m, 2H), 1.10 (d, J = 2.1 Hz, 10H).

[0170] Step 6. Synthesis of 5-((2S,3S)-3-amino-2-fluoro-3-(2-fluoro-5-methylphenyl)propyl)-1-(tetrahydro-2H-pyran-4-yl)pyrimidine-2, 4, 6 (1H, 3H, 5H)-trione (3G). A solution of crude 3F (1.3 g, 2.60 mmol) in ethanol (10 mL) was added thionyl chloride (334 mg) at 0 ^o C. After stirring at rt for 1 h, the reaction mixture was concentrated and the residue was dried in vacuo to give crude 3G (1.0 g) as a white solid, which was used for the next step without further purification. LC-MS (ES, m/z): 396 [M+H] ⁺ .

[0171] Step 7. Synthesis of (6S,7S)-6-fluoro-7-(2-fluoro-5-methylphenyl)-3-(tetrahydro-2H-pyran-4-yl)-5,6,7,8-tetrahydropyrido[2,3-d]pyrimidine-2, 4 (1H, 3H)-dione (3). A mixture of crude 3G (1.0 g, 2.53 mmol) in CH ₃ CN (15 mL) was put into a microwave reactor with stirring at 120 ^o C for 30 min. Subsequently, the mixture was concentrated and the residue was purified by preparative HPLC (column: C18 silica gel; mobile phase: CH3CN:H2O = 20:80 (v/v) increasing to CH3CN:H2O = 80:20 (v/v) within 40 min; detector: UV 254 nm) to give compound 3 (302 mg, 32%), as a white solid, which was identified as Form 1 polymorph (see Example 2). LC-MS (ES, m/z): 378 [M+H] ⁺ ; ¹ H NMR (300 MHz, d ⁶ -DMSO): d 10.20 (s, 1H), 7.38– 7.05 (m, 3H), 6.45 (s,1H), 5.11– 4.81 (m, 3H), 3.89 (dd, J = 10.8, 3.9 Hz, 2H), 3.34– 3.27 (m, 3H), 2.76–2.48 (m, 4H), 2.28 (s, 3H), 1.39–1.36 (m, 2H); ¹⁹ F NMR (376 MHz, d ⁶ -DMSO): d -123.51 (t, J = 86.5 Hz), -191.57 (d, J = 129.34 Hz).

PAT

• Tetrahydropyran (thp)-substituted bicyclic-pyrimidinedione compoundsPublication Number: EP-4464321-A2Priority Date: 2018-10-29
• Tetrahydropyran-substituted bicyclic pyrimidinedione compounds (THP)Publication Number: ES-2986923-T3Priority Date: 2018-10-29Grant Date: 2024-11-13
• Substituted 5,6,7,8-tetrahydropyrido[2,3-d]pyrimidine-2,4-diones for treating cardiac diseasesPublication Number: US-2024025894-A1Priority Date: 2018-10-29
• Substituted 5,6,7,8-tetrahydropyrido[2,3-d]pyrimidine-2,4-diones for treating cardiac diseasesPublication Number: US-12344607-B2Priority Date: 2018-10-29Grant Date: 2025-07-01
• Substituted 5,6,7,8-tetrahydropyrido[2,3-d]pyrimidine-2,4-diones for treating cardiac diseasesPublication Number: US-2025282779-A1Priority Date: 2018-10-29
• Tetrahydropyran (THP) Substituted Bicyclic Pyrimidinedione CompoundsPublication Number: CN-113056465-APriority Date: 2018-10-29
• Tetrahydropyrane (THP) -substituted bicyclic pyrimidinedione compoundsPublication Number: CN-119977963-APriority Date: 2018-10-29
• Tetrahydropyran (thp)-substituted bicyclic-pyrimidinedione compoundsPublication Number: EP-3873904-B1Priority Date: 2018-10-29Grant Date: 2024-07-10
• Substituted 5,6,7,8-tetrahydropyrido[2,3-d]pyrimidine-2,4-diones for treating cardiac diseasesPublication Number: US-11034693-B2Priority Date: 2018-10-29Grant Date: 2021-06-15
• Substituted 5,6,7,8-tetrahydropyrido[2,3-d]pyrimidine-2,4-diones for treating cardiac diseasesPublication Number: US-2022106314-A1Priority Date: 2018-10-29
• Tetrahydropyran (THP)-Substituted Bicyclic-Pyrimidinedione CompoundsPublication Number: JP-2024063091-APriority Date: 2018-10-29
• Tetrahydropyran (thp)-substituted bicyclic-pyrimidinedione compoundsPublication Number: TW-202426449-APriority Date: 2018-10-29
• Tetrahydropyrane (THP) -substituted bicyclic pyrimidinedione compoundsPublication Number: CN-113056465-BPriority Date: 2018-10-29Grant Date: 2025-01-28
• Tetrahydropyran (thp)-substituted bicyclic-pyrimidinedione compoundsPublication Number: US-2020165247-A1Priority Date: 2018-10-29
• BICYCLIC PYRIMIDINODIONA COMPOUNDS REPLACED WITH TETRAHYDROPYRAN, POLYMORPHIC FORM OF THE SAME AND THE USE OF THE SAME FOR THE TREATMENT OF HCMPublication Number: AR-116880-A1Priority Date: 2018-10-29
• Substituted 5,6,7,8-tetrahydropyrido[2,3-d]pyrimidine-2,4-diones for treating cardiac diseasesPublication Number: US-2022340569-A1Priority Date: 2018-10-29
• Tetrahydropyran (thp)-substituted bicyclic-pyrimidinedione compoundsPublication Number: EP-3873904-A1Priority Date: 2018-10-29
• CRYSTALLINE FORMS OF (6S,7S)-6-FLUORO-7-(2-FLUORO-5-METHYLPHENYL)- 3-(TETRAHYDRO-2H-PYRAN-4-YL)-5,6,7,8-TETRAHYDROPYRIDO[2,3- d]PYRIMIDINE-2,4(1H,3H)-DIONEPublication Number: WO-2024026058-A8Priority Date: 2022-07-29
• Crystalline forms of (6s,7s)-6-fluoro-7-(2-fluoro-5-methylphenyl)- 3-(tetrahydro-2h-pyran-4-yl)-5,6,7,8-tetrahydropyrido[2,3- d]pyrimidine-2,4(1h,3h)-dionePublication Number: EP-4561697-A1Priority Date: 2022-07-29
• Methods of Administering Myosin InhibitorsPublication Number: US-2023338378-A1Priority Date: 2022-04-26
• Methods of treatment with myosin modulatorPublication Number: US-2023158027-A1Priority Date: 2019-11-10
• tetrahydropyran-substituted bicyclic pyrimidinedione compounds (thp)Publication Number: BR-112021008077-A2Priority Date: 2018-10-29
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References

References

1.  Lehman, Sarah J.; Crocini, Claudia; Leinwand, Leslie A. (June 2022). "Targeting the sarcomere in inherited cardiomyopathies". Nature Reviews Cardiology. 19 (6): 353–363. doi:10.1038/s41569-022-00682-0. ISSN 1759-5010. PMC 9119933. PMID 35304599.
2.  Sebastian, Sneha Annie; Padda, Inderbir; Lehr, Eric J.; Johal, Gurpreet (September 2023). "Aficamten: A Breakthrough Therapy for Symptomatic Obstructive Hypertrophic Cardiomyopathy". American Journal of Cardiovascular Drugs. 23 (5): 519–532. doi:10.1007/s40256-023-00599-0. PMID 37526885. S2CID 260348901.
3.  Packard, Elizabeth; de Feria, Alejandro; Peshin, Supriya; Reza, Nosheen; Owens, Anjali Tiku (December 2022). "Contemporary Therapies and Future Directions in the Management of Hypertrophic Cardiomyopathy". Cardiology and Therapy. 11 (4): 491–507. doi:10.1007/s40119-022-00283-5. PMC 9652179. PMID 36243823.

////////delocamten, ANAX LAB, cardiac myosin inhibitor, MYK-224; BMS-986435, MYK 224, BMS 986435, IE5886BN8T

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