Olisutrigine bromide

 

Olisutrigine bromide

Cas 1393836-45-7

MF C25H35BrN2 MW443.5 g/mol

N-[2-[(2R)-1,1-dimethylpiperidin-1-ium-2-yl]ethyl]-N-(2-methylphenyl)-2,3-dihydro-1H-inden-2-amine bromide

(2R)-2-{2-[N-(2,3-dihydro-1H-inden-2-yl)-2-methylanilino]ethyl}-1,1-dimethylpiperidin-1-ium bromide
sodium channel blocker, analgesic, ASN008, ASN 008, EN 3427, 0M9Q318030

Olisutrigine bromide (also known as ASN-008 or EN3427) is an investigational, permanently charged sodium channel blocker being studied for its potent, long-lasting analgesic (pain-relieving) properties.

Key Characteristics

• Mechanism of Action: It acts as a membrane-impermeant sodium channel blocker. Because it carries a permanent cationic charge, it cannot easily cross healthy cell membranes on its own.
• Targeted Delivery: It often requires a "vehicle" or a combination drug (like lidocaine) to activate specific channels (such as TRP channels), allowing olisutrigine entry into pain-sensing neurons where it becomes entrapped and blocks pain signaling.
• Efficacy: Rodent pain models demonstrate that its analgesic effects are significantly longer-lasting than lidocaine alone.
• Chemical Profile: Its molecular formula is C₂₅H₃₅BrN₂ with a molecular weight of 443.5 g/mol, and its CAS registry number is 1393836-45-7.

Current Status

• Investigational Drug: It is not approved for human or veterinary medical use and remains in the research and development phase.
• Availability: It is strictly available as a reference standard compound for laboratory and preclinical research through chemical suppliers like MedChemExpress and BenchChem.

A Study to Evaluate the Anti-pruritic Effectiveness of ASN008 in Adults With Mild to Moderate Atopic Dermatitis

CTID: NCT05870865

Phase: Phase 2

Status: Completed

Date: 2025-05-16

SYN

https://patentscope.wipo.int/search/en/detail.jsf?docId=WO2012112969&_cid=P11-MRILQZ-81481-1

Example 43: General Procedure M - Preparation of (R)-1,1 -dimethyl-2-[2-((indan-2-yl)(2-methylphenyl)amino)ethyl]piperidinium bromide

Alcohol 37b was synthesized as previouslydescribed (Tetrahedron 2007, 63, 3000-3005)

To a 250 mL round bottom flask was charged 2-(2-hydroxyethyl)piperidine-1-carboxylic acid tert-butyl ester 37b (5.0 g, 21.80 mmol), dichloromethane (7.50 mL), a solution of KBr (0.52 g, 4.36 mmol) in 2.0 mL of water and TEMPO (0.1 g, 0.64 mmol). The mixture was cooled to about -5 °C. A solution of NaOCl (31.1 mL, 5.25%, 24.1 mmol) was added slowly over 20 minutes while maintaining the temperature at 0 °C. The mixture was further stirred at 0°C for 20 minutes. The organic layer was separated, and the aqueous layer was extracted with

dichloromethane. The combined dichloromethane extract was washed with water (50 mL), followed by brine. After drying over MgSO₄, the mixture was filtered and concentrated. The crude was purified with silica gel column chromatography to give product 38b (4.1 g, 83%) as colorless oil.

O

To a clean and dry 250 mL round bottom flask was charged sodium triacetoxyborohydride (5.59 g, 26.40 mmol), 4 A molecular sieves (10.0 g), amine 7e (7.37 g, 33.00 mmol) and dichloromethane (20.0 mL). The mixture was stirred and cooled to about 0 °C, and a solution of aldehyde 38b (5.0 g, 22.00 mmol) in 40 mL of dichloromethane was added. The mixture was then stirred further at 0 °C for about 1 hour and at ambient temperature for an additional 40 minutes. The reaction mixture was quenched with aqueous saturated NaHCO₃ (100 mL). After separation of organic layer, the mixture was extracted with dichloromethane. After drying over MgSO₄, the organic layer was concentrated. The crude product was purified by silica gel column chromatography to give product 40f (7.2 g, 75.3%) as colorless oil.

To a clean and dry 250 mL round bottom flask was charged lithium aluminum hydride (1.53 g, 40.27 mmol) and THF (30.0 mL). The mixture was heated to reflux. A solution of carbamate 40f (7.0 g, 16.11 mmol) in THF (40.0 mL) was added dropwise over 5 minutes. After refluxing for 15 h, the reaction mixture was cooled to 0 °C, and water (1.55 mL) was added slowly and carefully, followed by THF (100 mL) and 15% NaOH (1.55 mL). After stirring the mixture at room temperature for 1.0 h, MgSO₄ was added, and the mixture was stirred further for 15 minutes. The mixture was filtered and concentrated to obtain the crude product, which was purified by silica gel column chromatography to afford product 11e (4.7 g, 84%) as pale yellow oil. Optical purity by chiral HPLC: 99.3% ee.

To a clean and dry 250 mL round bottom flask was charged diamine 11e (4.70 g, 13.49 mmol) and 1.07 M bromomethane in MTBE (126.0 mL, 134.8 mmol). After stirring at room temperature for 20 h, the reaction mixture was filtered. The solid cake was washed with MTBE to give the product (4.40 g, 73%) as white powder. Optical purity by chiral HPLC: 99.3% ee.

PAT

https://patentscope.wipo.int/search/en/detail.jsf;jsessionid=53D672FEEE9931FFC5F125D61A00D7FA.wapp1nB?docId=WO2026050699&_cid=P11-MRILJW-76628-1

PAT

https://patentscope.wipo.int/search/en/detail.jsf?docId=WO2025250498&_cid=P11-MRILME-78328-1

Compound 1 is described in WO2012/112969, wherein Compound 1 is reported at Example 43, and certain formulations of Compound 1 are described in WO2020/113050,

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References

AMINOINDANE COMPOUNDS AND THEIR APPLICATION FOR THE TREATMENT OF PAIN

Publication Number: RU-2013142433-A

Priority Date: 2011-02-18

• Aminoindane compounds and use thereof in treating painPublication Number: US-8865741-B2Priority Date: 2011-02-18Grant Date: 2014-10-21
• Aminoindan compound and its use in treating painPublication Number: CN-107540599-BPriority Date: 2011-02-18Grant Date: 2021-06-04
• Aminoindane compounds and their use in the treatment of painPublication Number: ES-2675510-T3Priority Date: 2011-02-18Grant Date: 2018-07-11
• Aminoindane compounds and use thereof in treating painPublication Number: EP-2675787-B1Priority Date: 2011-02-18Grant Date: 2018-03-28
• AMINOINDANE COMPOUNDS AND THEIR APPLICATION FOR THE TREATMENT OF PAINPublication Number: RU-2016151688-APriority Date: 2011-02-18
• Aminoindane compounds and use thereof in treating painPublication Number: RU-2612959-C2Priority Date: 2011-02-18Grant Date: 2017-03-14
• AMINOINDAN COMPOUNDS AND USE THEREOF IN THE TREATMENT OF PAINPublication Number: DK-2675787-T3Priority Date: 2011-02-18Grant Date: 2018-07-16
• Load Aminoinden Compounds and Therapeutic Compounds Containing Them and Uses in the Treatment of Itching and PainPublication Number: IL-227967-APriority Date: 2011-02-18
• Aminoindane compounds and use thereof in treating painPublication Number: EP-3363437-B1Priority Date: 2011-02-18Grant Date: 2021-07-28
• Aminoindane compounds and use thereof in treating painPublication Number: KR-20200125765-APriority Date: 2011-02-18
• Aminoindane compounds and use thereof in treating painPublication Number: WO-2012112969-A1Priority Date: 2011-02-18
• Aminoindane compounds and use thereof in treating painPublication Number: CA-2826648-CPriority Date: 2011-02-18Grant Date: 2019-06-04
• Aminoindane compounds for use in treating urological painPublication Number: EP-3970723-A1Priority Date: 2011-02-18
• Aminoindane compounds and use thereof in treating painPublication Number: CA-2826648-A1Priority Date: 2011-02-18
• Aminoindane Compounds and Use Thereof in Treating PainPublication Number: US-2012214809-A1Priority Date: 2011-02-18
• Use of aminoindane compounds in treating overactive bladder and interstitial cystitisPublication Number: US-9044482-B2Priority Date: 2012-08-15Grant Date: 2015-06-02
• Aminoindane compounds and their use in the treatment of painPublication Number: ES-2898910-T3Priority Date: 2011-02-18Grant Date: 2022-03-09
• Aminoindane compounds and use thereof in treating painPublication Number: AU-2012219254-A1Priority Date: 2011-02-18
• Aminoindane compounds and use thereof in treating painPublication Number: EP-2675787-A1Priority Date: 2011-02-18
• Aminoindane compounds and use thereof in treating painPublication Number: EP-3363437-A1Priority Date: 2011-02-18
• 6-(4-Nitro-phenoxy)-2H-pyridazin-3-one and 6-(4-amino-phenoxy)-2H-pyridazin-3-one as intermediates of thyroid hormone analogs The preparation method of ketone derivativePublication Number: CN-116406356-APriority Date: 2020-10-23
• Use of Aminoindane Compounds in Treating Overactive Bladder and Interstitial CystitisPublication Number: US-2014051702-A1Priority Date: 2012-08-15
• Use of aminoindane compounds in treating overactive bladder and interstitial cystitisPublication Number: US-2015290182-A1Priority Date: 2012-08-15
• Use of aminoindane compounds in treating overactive bladder and interstitial cystitisPublication Number: US-9375423-B2Priority Date: 2012-08-15Grant Date: 2016-06-28
• Use of aminoindane compounds in treating overactive bladder and interstitial cystitisPublication Number: WO-2014028675-A1Priority Date: 2012-08-15

///////////olisutrigine bromide, anax labs, sodium channel blocker, analgesic, ASN008, ASN 008, EN 3427, 0M9Q318030

#olisutrigine bromide, #anax labs, #sodium channel blocker, #analgesic, #ASN008, #ASN 008, #EN 3427, #0M9Q318030

Ontunisertib

 

Ontunisertib

CAS 2647949-48-0

MFC27H21F2N5O MW469.5 g/mol

• 1H-Pyrazole-1-acetamide, N-[(2,6-difluorophenyl)methyl]-3-(6-methyl-2-pyridinyl)-4-(4-quinolinyl)-
• N-(2,6-Difluorobenzyl)-2-(3-(6-methylpyridin-2-yl)-4-(quinolin-4-yl)-1H-pyrazol-1-yl)acetamide

N-[(2,6-difluorophenyl)methyl]-2-[3-(6-methyl-2-pyridinyl)-4-quinolin-4-ylpyrazol-1-yl]acetamide

N-(2,6-difluorobenzyl)-2-(3-(6-methylpyridin-2-yl)-4-(quinolin-4-yl)-1H-pyrazol-1-yl)acetamide

N-[(2,6-difluorophenyl)methyl]-2-[3-(6-methylpyridin-2-yl)-4-(quinolin-4-yl)-1H-pyrazol-1-yl]acetamide
serine/threonine kinase inhibitor, AGMB 129, SF6HGC94LK

Ontunisertib (AGMB-129) is an experimental, orally active small-molecule drug developed by Agomab Therapeutics to treat Fibrostenosing Crohn’s Disease (FSCD). It acts as a highly selective inhibitor of ALK5 (also known as Transforming Growth Factor-beta type I receptor or TGF-β RI).

Mechanism of Action

• Local Targeting: Designed to act specifically within the gastrointestinal (GI) tract.
• High Tissue Exposure: Provides high local exposure in inflamed and scarred intestinal tissues.
• Liver Inactivation: Undergoes rapid first-pass metabolism in the liver immediately after GI absorption.
• Safety Feature: Converts into an inactive metabolite to prevent systemic exposure and avoid cardiac toxicity.

Clinical Development Status

• FDA Status: Granted Fast Track Designation by the U.S. FDA.
• Phase 2a Results: Successfully completed the STENOVA clinical trial. Results demonstrated excellent safety, high local tissue penetration, and positive structural improvements in bowel strictures.
• Phase 2b Trial: Enrolling patients for the global, 52-week NOV-ERA trial to test multiple doses against a placebo. The primary goal is assessing the endoscopically confirmed widening of narrowed intestinal strictures

• NOV-ERA - A Clinical Trial to Assess the Efficacy and Safety of Ontunisertib Compared to Placebo in Patients With Fibrostenosing Crohn's DiseaseCTID: NCT07683325Phase: Phase 2Status: Not yet recruitingDate: 2026-07-06
• Human Mass Balance Study of [14C] Ontunisertib in Healthy VolunteersCTID: NCT07672574Phase: Phase 1Status: Not yet recruitingDate: 2026-06-29
• A Multiple Ascending Dose Study With AGMB-129 in Healthy ParticipantsCTID: NCT07118878Phase: Phase 1Status: CompletedDate: 2025-11-21
• STENOVA - A Study to Evaluate Safety, Tolerability, PK and PD of AGMB-129 in Patients With Fibrostenotic Crohn's DiseaseCTID: NCT05843578Phase: Phase 2Status: Active, not recruitingDate: 2025-11-21
• Drug-Drug Interaction Study With AGMB-129 and Midazolam in Healthy ParticipantsCTID: NCT05937386Phase: Phase 1Status: CompletedDate: 2024-06-18

SYN

• US12297186, Example 24

SYN

[WO2021105317A1]

https://patentscope.wipo.int/search/en/detail.jsf?docId=WO2021105317&_cid=P20-MRPQUQ-14721-1

Example 24: N-(2,6-difluorobenzyl)-2-(3-(6-methylpyridin-2-yl)-4-(quinolin-4-yl)-1H-pyrazol-1 -yl)acetamide

¹H-NMR (300 MHz, DMSO-d₆): δ = 8.84 (d, J = 4.4 Hz, 1H), 8.76 (t, J = 5.3 Hz, 1H), 8.11-7.97 (m, 2H), 7.75-7.28 (m, 7H), 7.13 (t, J = 7.8 Hz, 2H), 6.97 (d, J = 7.5 Hz, 1 H), 4.99 (s, 2H), 4.43 (d, J = 5.3 Hz, 2H), 1.83 (s, 3H).

HPLC-MS: Rt 17.513 m/z 470.0 [M+H]⁺.

PAT

https://patentscope.wipo.int/search/en/detail.jsf?docId=WO2025176835&_cid=P20-MRPR39-19345-1

Potent inhibitors of TGFpRII-TGFpRI (ALK5) have been described in W02021/105317 including the compound (/V-(2,6-difluorobenzyl)-2-(3-(6-methylpyridin-2-yl)-4-(quinolin-4-yl)-1/7-pyrazol-1-yl)acetamide) which is the compound of formula (I) as shown below (see Example 24):

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References

///////////ontunisertib, anax labs, serine/threonine kinase inhibitor, AGMB 129, SF6HGC94LK

#ontunisertib, #anax labs, #serine/threonine kinase inhibitor, #AGMB 129, #SF6HGC94LK

Opakalim

 

Opakalim

CAS 2376397-93-0

MF C18H22F2N4O MW 348.4 g/mol

N-(1-tert-butyl-6-cyano-4,7-difluorobenzimidazol-2-yl)-3,3-dimethylbutanamide

• N-(1-tert-butyl-6-cyano-4,7-difluorobenzimidazol-2-yl)-3,3-dimethylbutanamide
• Butanamide, N-[6-cyano-1-(1,1-dimethylethyl)-4,7-difluoro-1H-benzimidazol-2-yl]-3,3-dimethyl-
• N-[6-Cyano-1-(1,1-dimethylethyl)-4,7-difluoro-1H-benzimidazol-2-yl]-3,3-dimethylbutanamide

N-(1-tert-butyl-6-cyano-4,7-difluoro-1H-1,3-benzimidazol-2-yl)-3,3-dimethylbutanamide
potassium channel activator, antiepileptic, BHV-7000; BHV7 000, BPN-25203, BPN 25203, KB-3061, KB 3061, 73H9J7RBA2

BHV-7000 is under investigation in clinical trial NCT06419608 (Efficacy and Safety Study of BHV-7000 Monotherapy in Major Depression).

Opakalim (also known as BHV-7000) is an investigational, small-molecule medication that acts as a selective activator of Kv7.2 and Kv7.3 potassium channels. Developed by Biohaven Pharmaceuticals, it targets a clinically validated pathway to regulate neuronal hyperexcitability, primarily for the treatment of epilepsy and focal seizures.

Key Characteristics

• Mechanism of Action: It opens Kv7.2/7.3 potassium channels. This stabilizes electrical activity in the brain. Unlike older class drugs, it has minimal to no (GABA_A) receptor activity.
• Safety Benefit: Its precision prevents typical central nervous system side effects. Patients experience much lower rates of somnolence, fatigue, and severe dizziness compared to other anti-seizure medications.
• Administration: It is taken orally once a day. It requires no titration period before reaching therapeutic dosing.

Current Clinical Status

• Refractory Focal Epilepsy: The drug is undergoing phase 2/3 clinical evaluation. The pivotal RISE 3 study completed patient enrollment, with high-profile top-line efficacy data anticipated in the second half of 2026.
• Idiopathic Generalized Epilepsy (IGE): Recent clinical data highlights a three-fold prolongation in the time to a second generalized tonic-clonic seizure compared to a placebo.
• Other Explored Indications: While it is actively tested for conditions like bipolar disorder and erythromelalgia (pain), an exploratory phase 2 trial for major depressive disorder failed to meet its primary goals.

Opakalim (INNTooltip International Nonproprietary Name, USANTooltip United States Adopted Name; developmental code names BHV-7000, BPN-25203, and KB-3061) is a highly selective K_v7.2 and K_v7.3 potassium channel opener which is under development for the treatment of bipolar disorders, epilepsy, partial epilepsies, major depressive disorder, erythromelalgia, pain, infantile spasms, and mood disorders.^[1][2][3][4] It is taken orally.^[1] The drug was originated by Channel Biosciences and was under development by Biohaven Pharmaceuticals or Biohaven Therapeutics.^[1][2] As of April 2026, it is in phase 2/3 clinical trials for bipolar disorders, epilepsy, and partial epilepsies, phase 2 trials for major depressive disorder, and phase 1 trials for erythromelalgia and pain, whereas no recent development has been reported for infantile spasms and mood disorders.^[1][2] A phase 2 trial for major depressive disorder failed to meet its primary efficacy endpoint, resulting in focus more on epilepsy instead.^[3]

• Study to Determine if BHV-7000 is Effective and Safe in Adults With Refractory Focal Onset EpilepsyCTID: NCT06309966Phase: Phase 2/Phase 3Status: Active, not recruitingDate: 2026-07-01
• A Study to Determine if BHV-7000 is Effective and Safe in Adults With Refractory Focal Onset EpilepsyCTID: NCT06132893Phase: Phase 2/Phase 3Status: RecruitingDate: 2026-05-01
• Long-term Safety and Tolerability of BHV-7000CTID: NCT06443463Phase: Phase 2Status: Enrolling by invitationDate: 2026-05-01
• A Phase 1b Study of BHV-7000 in Participants With Inherited ErythromelalgiaCTID: NCT07262268Phase: Phase 1Status: Enrolling by invitationDate: 2026-04-08
• Long-term Safety Study of BHV-7000 in Participants With Major Depressive Disorder (MDD)CTID: NCT06423781Phase: Phase 2Status: CompletedDate: 2026-04-01
• A Study to Determine if BHV-7000 is Effective and Safe in Adults With Idiopathic Generalized Epilepsy With Generalized Tonic-clonic SeizuresCTID: NCT06425159Phase: Phase 2/Phase 3Status: TerminatedDate: 2026-03-24
• Efficacy and Safety Study of BHV-7000 Monotherapy in Major DepressionCTID: NCT06419608Phase: Phase 2Status: CompletedDate: 2026-01-07
• BHV-7000 Acute Treatment of Bipolar ManiaCTID: NCT06419582Phase: Phase 2/Phase 3Status: CompletedDate: 2025-12-16
• BHV-7000 Open-Label Extension Bipolar Mania StudyCTID: NCT06423794Phase: Phase 2Status: TerminatedDate: 2025-12-16

PAT

[US20230000831]

https://patentscope.wipo.int/search/en/detail.jsf?docId=US383826737&_cid=P20-MRSLRP-32698-1

PAT

https://patentscope.wipo.int/search/en/detail.jsf?docId=WO2025035066&_cid=P20-MRSLVM-39325-2

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References

• Kv7 channel activators compositions and methods of usePublication Number: US-11724990-B2Priority Date: 2018-03-19Grant Date: 2023-08-15
• KV7 channel activators compositions and methods of usePublication Number: US-12286408-B2Priority Date: 2018-03-19Grant Date: 2025-04-29
• KV7 channel activators compositions and methods of usePublication Number: US-11261162-B2Priority Date: 2018-03-19Grant Date: 2022-03-01
• Kv7 channel activators compositions and methods of usePublication Number: US-2019284142-A1Priority Date: 2018-03-19
• Kv7 channel activators compositions and methods of usePublication Number: US-10851067-B2Priority Date: 2018-03-19Grant Date: 2020-12-01
• KV7 channel activator composition and method of use thereofPublication Number: KR-20200133259-APriority Date: 2018-03-19
• Kv7 channel activators compositions and methods of usePublication Number: US-2021130299-A1Priority Date: 2018-03-19
• KV7 channel activator composition and method of use thereofPublication Number: KR-102731128-B1Priority Date: 2018-03-19Grant Date: 2024-11-18
• Methods of use for kv7 channel activatorsPublication Number: US-2025312316-A1Priority Date: 2019-09-17
• Methods of use for KV7 channel activatorsPublication Number: US-12370176-B2Priority Date: 2019-09-17Grant Date: 2025-07-29
• How to use KV7 channel activatorPublication Number: CN-118986972-APriority Date: 2019-09-17
• Kv7 channel activators compositions and methods of usePublication Number: US-2024002349-A1Priority Date: 2018-03-19
• Kv7 channel activators compositions and methods of usePublication Number: US-2023000831-A1Priority Date: 2018-03-19

References

1.  "Biohaven Pharmaceuticals". AdisInsight. 15 April 2026. Retrieved 31 May 2026.
2.  "Delving into the Latest Updates on Opakalim with Synapse". Synapse. 2 April 2026. Retrieved 31 May 2026.
3.  Pelorosso C, Balestrini S, Guerrini R (May 2026). "Potassium channel agonists emerging as treatment options for focal epilepsy: are we breaking new ground?". Expert Opinion on Emerging Drugs: 1–8. doi:10.1080/14728214.2026.2675274. hdl:2158/1473832. PMID 42153277.
4.  Pong AW (December 2025). "Expanding the toolkit: An update on the evolution of new therapies for Lennox-Gastaut Syndrome". Seminars in Pediatric Neurology. 56 101242. doi:10.1016/j.spen.2025.101242. PMID 41371876.

Clinical data
Other names	BHV-7000; BHV7000; BPN-25203; BPN25203; KB-3061; KB3061
Routes of administration	Oral[1]
Drug class	Kv7.2 and Kv7.3 potassium channel opener
Identifiers
IUPAC name
CAS Number	2376397-93-0
PubChem CID	139487180
DrugBank	DB22041
ChemSpider	129910012
UNII	73H9J7RBA2
KEGG	D13061
Chemical and physical data
Formula	C18H22F2N4O
Molar mass	348.398 g·mol−1
3D model (JSmol)	Interactive image
SMILES
InChI

////////opakalim, anax labs, potassium channel activator, antiepileptic, BHV-7000; BHV7 000, BPN-25203, BPN 25203, KB-3061, KB 3061, 73H9J7RBA2

#opakalim, #anax labs, #potassium channel activator, #antiepileptic, #BHV-7000, #BHV7 000, #BPN-25203, #BPN 25203, #KB-3061, K#B 3061, #73H9J7RBA2

Gedatolisib

 

Gedatolisib

Approvals 3026, FDA 2026, 7/14/2026, Revtorpyk

PF-05212384; PF-5212384; PKI-587 CAS 1197160-78-3 Chemical Formula: C32H41N9O4 Molecular Weight: 615.72 1-(4-{[4-(Dimethylamino)-1-piperidinyl]carbonyl}phenyl)-3-{4-[4,6-di(4-morpholinyl)-1,3,5-triazin-2-yl]phenyl}urea 3-{4-[bis(morpholin-4-yl)-1,3,5-triazin-2-yl]phenyl}-1-{4-[4-(dimethylamino)piperidine-1-carbonyl]phenyl}urea N-[4-[[4-(Dimethylamino)-1-piperidinyl]carbonyl]phenyl]-N'-[4-[4,6-di(4-morpholinyl)-1,3,5-triazin-2-yl]phenyl]urea гедатолисиб [Russian] [INN] غيداتوليسيب [Arabic] [INN] 吉达利塞 [Chinese] [INN]

1-(4-(4-(Dimethylamino)piperidine-1-carbonyl)phenyl)-3-(4-(4,6-dimorpholino-1,3,5-triazin-2-yl)phenyl)urea

Urea, N-[4-[[4-(dimethylamino)-1-piperidinyl]carbonyl]phenyl]-N'-[4-(4,6-di-4-morpholinyl-1,3,5-triazin-2-yl)phenyl]-

96265TNH2R

In combination with fulvestran, to treat hormone receptor-positive, human epidermal growth factor receptor 2-negative, locally advanced or metastatic breast cancer without a PIK3CA mutation detected following progression on or after treatment with at least one line of endocrine therapy in the metastatic setting

Gedatolisib, sold under the brand name Revtorpyk, is an anti-cancer drug used for the treatment of breast cancer.^[1] It is under development by Celcuity, Inc. Gedatolisib is a kinase inhibitor.^[1] The mechanism of action is accomplished by binding the different p110 catalytic subunit isoforms of PI3K and the kinase site of mTOR.^[2] Gedatolisib is administered by intravenous infusion.^[1]

Gedatolisib was approved for medical use in the United States in July 2026.^[1][3]

Medical uses

Gedatolisib is indicated in combination with fulvestrant, with or without palbociclib, for the treatment of adults with hormone receptor (HR)-positive, human epidermal growth factor receptor 2 (HER2)-negative locally advanced or metastatic breast cancer without a PIK3CA mutation detected following progression on or after treatment with at least one line of endocrine therapy in the metastatic setting.^[1]

• Synthesis of New Dialkyl 2,2′-[Carbonylbis(azanediyl)]dibenzoates via Curtius RearrangementDOI: 10.1055/s-0040-1706643Publication Date: 2021Publication Name: Synthesis
• A New One-Pot Three-Component Synthesis of 4-Aryl-6-cycloamino-1,3,5-triazin-2-amines under Microwave IrradiationDOI: 10.1055/a-1401-2795Publication Date: 2021Publication Name: Synthesis

PAT

https://patentscope.wipo.int/search/en/detail.jsf?docId=US42900900&_cid=P22-MRVGV9-51327-1

Example 76

Preparation of 1-(4-(4-(dimethylamino)piperidine-1-carbonyl)phenyl)-3-(4-(4,6-dimorpholino-1,3,5-triazin-2-yl)phenyl)urea

To the solution of 4-(3-(4-(4,6-dimorpholino-1,3,5-triazin-2-yl)phenyl)ureido)benzoic acid (50 mg; 0.099 mmol), Hunig's base (103 μL, 0.594 mmol), HBTU (188 mg, 0.495 mmol) in 2 mL of NMP was reacted according to example 68 with N,N-dimethylpiperidin-4-amine (51 mg, 0.396 mmol). Evaporated the solvent and purified by HPLC to give the product (30.6 mg, 52% yield); MS (ESI) m/z=616.7.

PATENT

https://patentscope.wipo.int/search/en/detail.jsf?docId=WO2010096619&_cid=P22-MRVGV9-51327-1

Scheme 1

Preparation of 1-(4-(4-(dimethylamino) piperidine-1-carbonyl)phenyl-3-(4-(4,6- dimorpholino-1 ,3,5-triazine-2-yl)phenyl) urea (9)

To a slurry of 4-(3-(4-(4,6-dimorpholino-1 ,3,5-triazine-2- yl)phenyl)ureido)benzoic acid (7, 45.5 g, 0.09 mol) in dry THF (1.6 L) heated to 50 ⁰C was added N,N'-carbonyl diimidazole (28 g, 0.17 mol). The reaction mixture was heated for 2 hours and followed by dimethylaminopiperidine (8, 23.5 g, 0.18 mol) and stirred at 53 ⁰C for 16 hours. The reaction mixture was cooled to the room temperature and filtered. The cake was washed with 2-propanol and air-dried to give 97 % pure white powder in 88% yield (49.2 g, 0.08 mol). To the solids stirred in dimethyl acetamide (DMAC, 165 ml) at 70° C for 1 hour was added 2-propanol (640 ml) and the mixture was stirred at 65 ⁰C for additional 1 hour. The solids were filtered, washed with 2-propanol and dried in a vacuum oven at 70⁰C for 16 hour to give crystalline white powder (45 g) with >99% purity. The above-mentioned work up process and crystallization procedure gave a Pd residue of 20 ppm. Alternate procedures for the formation of 1-(4-(4-(dimethylamino) piperidine-1 - carbonyl)phenyl-3-(4-(4,6-dimorpholino-1 ,3,5-triazine-2-yl)phenyl) urea (9)

To the solution of 4-(4,6-dimorpholin-4-yl-1 ,3,5-triazin-2-yl) aniline (4, 18 g, 0.052 mol) in dichloromethane (300 ml) was added methyl 4-isocyanato benzoate (5, 10.5 g, 0.061 mol) and the reaction mixture was stirred for 5 hours. The separated solids were filtered, washed with ether and air dried to give beige solids (21 g, 0.04 mol). Yield 77%. 90 % pure by HPLC; Mass: 520.1 (M+H). Preparation of 4-(3-(4-(4,6-dimorpholino-1 ,3,5-triazine-2-yl)phenyl)ureido) benzoic acid (7)

The mixture of methyl 4-(3-(4-(4,6-dimorpholino-1 ,3,5-triazine-2-yl)ureido)benzoate (6, 21 g, 0.04mol) and lithium hydroxide monohydrate (3.8 g, 0.09 mol) in THF (120 ml), MeOH (60 ml), and water (60 ml) was heated at 80 ⁰C for 3 hours. The dark brown solution was cooled to room temperature and made acidic with concentrated HCI. The solids were filtered, washed with water, washed with acetone , washed with ether, and dried in a vacuum oven at 60 ⁰C for 48 hours to give off white solids of 4-(3-(4-(4,6-dimorpholino-1 ,3,5-triazine-2-yl)phenyl)ureido) benzoic acid (19.2 g, 0.038 mol). Mass: 506.3 (M+H)⁺; Yield.94%. 1 -(4-(4-(dimethylamino) piperidine-1 -carbonyl)phenyl-3-(4-(4,6-dimorpholino- 1 ,3,5-triazine-2-yl)phenyl) urea (9)

The suspension of 4-(3-(4-(4,6-dimorpholino-1 ,3,5-triazine-2-yl)phenyl)ureido) benzoic acid (7, 17 g, 33.66 mmol) and N-(3-dimethylaminopropyl)ethyl carbodiimide hydrochloride (9.5 g, 49.5 mmol) in THF (200 ml) and acetonitrile (50 ml) was stirred for 10 min and followed by addition of 1-hydroxybenzotriazole hydrate (6.4 g, 47.88 mmol). The reaction mixture was stirred for 30 min and 4-dimethylaminopiperidine (8, 8.86 g, 69.2 mmol) was added by drops. After being stirred for additional 16 hours, the reaction mixture was concentrated to min. The solids were filtered and washed thoroughly with water (very fine suspension). The cake was slurred in hot ethanol, filtered and dried in a vacuum oven at 68 ⁰C for 16 hours to give off white solids (10.3 g, 16.77 mmol). M. p. 238-240 ⁰C. 99 % pure. Mass: 616.3 (M+H)⁺; Yield 50 %.

PATENT

WO 2009143317

WO 2010096619

WO 2012148540

WO 2014151147

PATENT

US 20170119778

PAPER

Journal of Medicinal Chemistry (2010), 53(6), 2636-2645

http://pubs.acs.org/doi/abs/10.1021/jm901830p

J. Med. Chem., 2010, 53 (6), pp 2636–2645

DOI: 10.1021/jm901830p

Abstract

The PI3K/Akt signaling pathway is a key pathway in cell proliferation, growth, survival, protein synthesis, and glucose metabolism. It has been recognized recently that inhibiting this pathway might provide a viable therapy for cancer. A series of bis(morpholino-1,3,5-triazine) derivatives were prepared and optimized to provide the highly efficacious PI3K/mTOR inhibitor 1-(4-{[4-(dimethylamino)piperidin-1-yl]carbonyl}phenyl)-3-[4-(4,6-dimorpholin-4-yl-1,3,5-triazin-2-yl)phenyl]urea 26 (PKI-587). Compound 26 has shown excellent activity in vitro and in vivo, with antitumor efficacy in both subcutaneous and orthotopic xenograft tumor models when administered intravenously. The structure−activity relationships and the in vitro and in vivo activity of analogues in this series are described.

Preparation of 1-(4-{[4-(Dimethylamino)piperidin-1-yl]carbonyl}phenyl)-3-[4-(4,6-dimorpholin-4- yl-1,3,5-triazin-2-yl)phenyl]urea (26)

MS (ESI) m/z = 616.7. HRMS: calcd for C₃₂H₄₁N₉O₄ + H⁺, 616.335 43; found (ESI-FTMS, [M + H]⁺), 616.334 24. Purity by analytical HPLC 99.3%. (Prodigy ODS3, 0.46 cm × 15 cm, 20 min gradient acetonitrile in water, trifluoroacetic acid, detector wavelengths, 215 and 254 nm.) ¹H NMR (DMSO-d₆) δ 1.29−1.36 (m, 6H), 2.6 (m, 4H), 2.9 (m,1H), 3.3 (m, 4H), 3.6 (m, 8H), 3.7 (m, 8H), 7.3 (d, J = 8.3 Hz, 2H), 7.51−7.57 (m, 4H), 8.3 (d, J = 8.3 Hz 2H), 8.9 (s, 1H), 9.0 (s, 1H) ppm. Anal. Calcd for C₃₂H₄₁N₉O₄: C 62.42%, H 6.71%, N 20.47%. Found: C 62.34%, H 6.67%, N 20.39%.

PAPER

Bioorganic & Medicinal Chemistry Letters (2011), 21(16), 4773-4778.

http://www.sciencedirect.com/science/article/pii/S0960894X11008468

PAPER

New and Practical Synthesis of Gedatolisib

http://pubs.acs.org/doi/10.1021/acs.oprd.7b00298

Org. Process Res. Dev., Article ASAP

DOI: 10.1021/acs.oprd.7b00298

Abstract

A new, practical, and convergent synthetic route of gedatolisib, an antitumor agent, is developed on a hectogram scale which avoids the Pd coupling method. The key step is adopting 6-(4-nitrophenyl)-1,3,5-triazine-2,4-diamine and 2,2′-dichlorodiethyl ether to prepare the key 4,4′-(6-(4-nitrophenyl)-1,3,5-triazine-2,4-diyl)dimorpholine in 77% yield and 98.8% purity. Gedatolisib is obtained in 48.6% yield over five simple steps and 99.3% purity (HPLC). Purification methods of the intermediates and the final product involved in the route are given.

off-white solid. ¹H NMR (400 MHz, DMSO-d₆): δ 1.46 (brs, 2H), 1.89 (brs, 2H), 2.29 (s, 6H), 2.94 (brs, 2H), 3.76 (m, 8H), 3.89 (m, 8H), 7.09 (d, J = 8.4 Hz, 2H), 7.20 (d, J = 8.4 Hz, 2H), 7.50 (d, J = 8.7 Hz, 2H), 8.28 (s, 1H), 8.31 (d, J = 8.6 Hz, 2H), 8.48 (s, 1H). ESI-MS (m/z) 615.9 (M + H). HPLC conditions: Column: Agilent Eclipse XDB-C18 (250 mm × 4.6 mm × 5 μm); Detection: 254 nm; Flow rate: 0.8 mL/min; Temperature: 30 °C; Injection load: 1 μL; Solvent: MeOH; Concentration: 0.5 mg/mL; Run time: 20 min; Mobile phase A: water; Mobile phase B: MeOH/TEA = 100:0.1; Gradient program: time (min): 20; % of mobile phase A: 10; % of mobile phase B: 90; t_R = 2.598 min, purity: 99.34%

• Zhao, X.; Tan, Q.; Zhang, Z.; Zhao, Y. Med. Chem. Res. 2014, 23, 5188– 5196 DOI: 10.1007/s00044-014-1084-z
• Khafizova, G.; Potoski, J. R. PCT Int. Appl. WO 2010096619, 2010.
• Venkatesan, A. M.; Chen, Z.; Dehnhardt, C. M.; Dos Santos, O.; Delos Santos, E. G.; Zask, A.; Verheijen, J. C.; Kaplan, J. A.; Richard, D. J.; Ayral-Kaloustian, S.; Mansour, T. S.; Gopalsamy, A.; Curran, K. J.; Shi, M. PCT Int. Appl. WO 2009143317, 2009.

REFERENCES

1: Gedaly R, Galuppo R, Musgrave Y, Angulo P, Hundley J, Shah M, Daily MF, Chen C, Cohen DA, Spear BT, Evers BM. PKI-587 and sorafenib alone and in combination on inhibition of liver cancer stem cell proliferation. J Surg Res. 2013 Nov;185(1):225-30. doi: 10.1016/j.jss.2013.05.016. Epub 2013 May 25. PubMed PMID: 23769634.

2: Gedaly R, Angulo P, Hundley J, Daily MF, Chen C, Evers BM. PKI-587 and sorafenib targeting PI3K/AKT/mTOR and Ras/Raf/MAPK pathways synergistically inhibit HCC cell proliferation. J Surg Res. 2012 Aug;176(2):542-8. doi: 10.1016/j.jss.2011.10.045. Epub 2011 Nov 21. PubMed PMID: 22261591.

3: Dehnhardt CM, Venkatesan AM, Chen Z, Delos-Santos E, Ayral-Kaloustian S, Brooijmans N, Yu K, Hollander I, Feldberg L, Lucas J, Mallon R. Identification of 2-oxatriazines as highly potent pan-PI3K/mTOR dual inhibitors. Bioorg Med Chem Lett. 2011 Aug 15;21(16):4773-8. doi: 10.1016/j.bmcl.2011.06.063. Epub 2011 Jun 21. PubMed PMID: 21763134.

4: Mallon R, Feldberg LR, Lucas J, Chaudhary I, Dehnhardt C, Santos ED, Chen Z, dos Santos O, Ayral-Kaloustian S, Venkatesan A, Hollander I. Antitumor efficacy of PKI-587, a highly potent dual PI3K/mTOR kinase inhibitor. Clin Cancer Res. 2011 May 15;17(10):3193-203. doi: 10.1158/1078-0432.CCR-10-1694. Epub 2011 Feb 15. PubMed PMID: 21325073.

5: Venkatesan AM, Chen Z, dos Santos O, Dehnhardt C, Santos ED, Ayral-Kaloustian S, Mallon R, Hollander I, Feldberg L, Lucas J, Yu K, Chaudhary I, Mansour TS. PKI-179: an orally efficacious dual phosphatidylinositol-3-kinase (PI3K)/mammalian target of rapamycin (mTOR) inhibitor. Bioorg Med Chem Lett. 2010 Oct 1;20(19):5869-73. doi: 10.1016/j.bmcl.2010.07.104. Epub 2010 Jul 30. PubMed PMID: 20797855.

6: Venkatesan AM, Dehnhardt CM, Delos Santos E, Chen Z, Dos Santos O, Ayral-Kaloustian S, Khafizova G, Brooijmans N, Mallon R, Hollander I, Feldberg L, Lucas J, Yu K, Gibbons J, Abraham RT, Chaudhary I, Mansour TS. Bis(morpholino-1,3,5-triazine) derivatives: potent adenosine 5'-triphosphate competitive phosphatidylinositol-3-kinase/mammalian target of rapamycin inhibitors: discovery of compound 26 (PKI-587), a highly efficacious dual inhibitor. J Med Chem. 2010 Mar 25;53(6):2636-45. doi: 10.1021/jm901830p. PubMed PMID: 20166697.

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References

• PRMT5 inhibitors and uses thereofPublication Number: US-12448388-B2Grant Date: 2025-10-21
• KRAS G12D modulating compoundsPublication Number: US-12448400-B2Grant Date: 2025-10-21
• TRIAZINE COMPOUNDS AS P13 KINASE AND MTOR INHIBITORSPublication Number: PT-2294072-TPriority Date: 2008-05-23
• TRIASINE UNITS AS P13 KINASE INHIBITORS AND MOTORPublication Number: ME-01111-BPriority Date: 2008-05-23
• HER2 mutation inhibitorsPublication Number: US-12447153-B2Grant Date: 2025-10-21
• Anti-hiv compoundsPublication Number: US-2025326779-A1
• Aryl aminopyrimidines as dual MerTK and TYRO3 inhibitors and methods thereofPublication Number: US-12448365-B2Grant Date: 2025-10-21

References

1.  https://celcuity.com/revtorpyk/REVTORPYK_PI_2026.pdf
2.  Dehnhardt CM, Venkatesan AM, Chen Z, Delos-Santos E, Ayral-Kaloustian S, Brooijmans N, et al. (August 2011). "Identification of 2-oxatriazines as highly potent pan-PI3K/mTOR dual inhibitors". Bioorganic & Medicinal Chemistry Letters. 21 (16): 4773–8. doi:10.1016/j.bmcl.2011.06.063. PMID 21763134.
3.  "FDA approves gedatolisib with fulvestrant, with or without palbociclib, for HR-positive, HER2-negative locally advanced or metastatic breast cancer". U.S. Food and Drug Administration (FDA). 14 July 2026. Retrieved 20 July 2026.  This article incorporates text from this source, which is in the public domain.
4.  Sabatini DM (November 2017). "Twenty-five years of mTOR: Uncovering the link from nutrients to growth". Proceedings of the National Academy of Sciences of the United States of America. 114 (45): 11818–11825. Bibcode:2017PNAS..11411818S. doi:10.1073/pnas.1716173114. PMC 5692607. PMID 29078414.
5.  Tian T, Li X, Zhang J (February 2019). "mTOR Signaling in Cancer and mTOR Inhibitors in Solid Tumor Targeting Therapy". International Journal of Molecular Sciences. 20 (3): 755. doi:10.3390/ijms20030755. PMC 6387042. PMID 30754640.
6.  Hua H, Kong Q, Zhang H, Wang J, Luo T, Jiang Y (July 2019). "Targeting mTOR for cancer therapy". Journal of Hematology & Oncology. 12 (1) 71. doi:10.1186/s13045-019-0754-1. PMC 6612215. PMID 31277692.
7.  Vanhaesebroeck B, Perry MW, Brown JR, André F, Okkenhaug K (October 2021). "PI3K inhibitors are finally coming of age". Nature Reviews. Drug Discovery. 20 (10): 741–769. doi:10.1038/s41573-021-00209-1. PMC 9297732. PMID 34127844. S2CID 235437841.
8.  Millis SZ, Ikeda S, Reddy S, Gatalica Z, Kurzrock R (December 2016). "Landscape of Phosphatidylinositol-3-Kinase Pathway Alterations Across 19 784 Diverse Solid Tumors". JAMA Oncology. 2 (12): 1565–1573. doi:10.1001/jamaoncol.2016.0891. PMID 27388585.
9.  Anderson EJ, Mollon LE, Dean JL, Warholak TL, Aizer A, Platt EA, et al. (2020). "A Systematic Review of the Prevalence and Diagnostic Workup of PIK3CA Mutations in HR+/HER2- Metastatic Breast Cancer". International Journal of Breast Cancer. 2020 3759179. doi:10.1155/2020/3759179. PMC 7322582. PMID 32637176.
10.  Clinical trial number NCT01420081 for "A Study Of Two Dual PI3K/mTOR Inhibitors, PF-04691502 And PF-05212384 In Patients With Recurrent Endometrial Cancer" at ClinicalTrials.gov
11.  Clinical trial number NCT01925274 for "A Study Of PF-05212384 Plus Irinotecan Vs Cetuximab Plus Irinotecan In Patients With KRAS And NRAS Wild Type Metastatic Colorectal Cancer" at ClinicalTrials.gov
12.  Clinical trial number NCT02438761 for "PF-05212384 (PKI-587) for t-AML/MDS or de Novo Relapsed or Refractory Acute Myeloid Leukemia (AML)" at ClinicalTrials.gov
13.  Clinical trial number NCT03698383 for "Phase II Study of Herzuma® Plus Gedatolisib in Patients With HER-2 Positive Metastatic Breast Cancer" at ClinicalTrials.gov
14.  Clinical trial number NCT03911973 for "Gedatolisib Plus Talazoparib in Advanced Triple Negative or BRCA1/2 Positive, HER2 Negative Breast Cancers" at ClinicalTrials.gov
15.  Clinical trial number NCT03065062 for "Study of the CDK4/6 Inhibitor Palbociclib (PD-0332991) in Combination With the PI3K/mTOR Inhibitor Gedatolisib (PF-05212384) for Patients With Advanced Squamous Cell Lung, Pancreatic, Head & Neck and Other Solid Tumors" at ClinicalTrials.gov
16.  Clinical trial number NCT02626507 for "Phase I Study of Combination of Gedatolisib With Palbociclib and Faslodex in Patients With ER+/HER2- Breast Cancer" at ClinicalTrials.gov
17.  "Celcuity Announces FDA Approval of Revtorpyk (gedatolisib) for the Treatment of HR+/HER2-, PIK3CA Wild-Type Locally Advanced or Metastatic Breast Cancer" (Press release). Celcuity. 14 July 2026. Retrieved 20 July 2026 – via GlobeNewswire.
18.  World Health Organization (2015). "International nonproprietary names for pharmaceutical substances (INN): recommended INN: list 73". WHO Drug Information. 29 (1). hdl:10665/331088.

External links

• Clinical trial number NCT05501886 for "Gedatolisib Plus Fulvestrant With or Without Palbociclib vs Standard-of-Care for the Treatment of Patients With Advanced or Metastatic HR+/HER2- Breast Cancer (VIKTORIA-1) (VIKTORIA-1)" at ClinicalTrials.gov

Clinical data
Trade names	Revtorpyk
Other names	PF-05212384; PKI-587
AHFS/Drugs.com	revtorpyk
License data	US DailyMed: Gedatolisib
Routes of administration	Intravenous infusion
Drug class	Antineoplastic
ATC code	None
Legal status
Legal status	US: ℞-only[1]
Identifiers
IUPAC name
CAS Number	1197160-78-3
PubChem CID	44516953
IUPHAR/BPS	7940
DrugBank	DB11896
ChemSpider	24644946
UNII	96265TNH2R
KEGG	D10635
ChEMBL	ChEMBL592445
CompTox Dashboard (EPA)	DTXSID40152557
Chemical and physical data
Formula	C32H41N9O4
Molar mass	615.739 g·mol−1
3D model (JSmol)	Interactive image
SMILES

/////////Gedatolisib, anax labs, approvals 3026, FDA 2026, PF 05212384, PF 5212384, PKI-587, PF-05212384, PF-5212384, PKI 587, gedatolisib, antitumor agent, PHASE 3, PFIZER, гедатолисиб , غيداتوليسيب , 吉达利塞 , 96265TNH2R

O=C(NC1=CC=C(C2=NC(N3CCOCC3)=NC(N4CCOCC4)=N2)C=C1)NC5=CC=C(C(N6CCC(N(C)C)CC6)=O)C=C5

 Journal of Medicinal Chemistry (2017), 60(17), 7524-7538 PQR 309

#Gedatolisib, #anax labs, #approvals 3026, #FDA 2026, #PF 05212384, #PF 5212384, #PKI-587, #PF-052123842, #PF-5212384; #PKI 587, #gedatolisib, #antitumor agent, #PHASE 3, #PFIZER, #гедатолисиб , #غيداتوليسيب , #吉达利塞 , #96265TNH2R