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Rosolutamide
Rosolutamide
CAS 1039760-91-2
MF C28H32O6 MW464.5 g/mol
(1E,6E)-4-(cyclobutylmethyl)-1,7-bis(3,4-dimethoxyphenyl)hepta-1,6-diene-3,5-dione
(1E,6E)-4-(cyclobutylmethyl)-1,7-bis(3,4-dimethoxyphenyl)hepta-1,6-diene-3,5-dione
antiandrogen, ASC-JM-17, ASC-JM17, JM17, ALZ-003, ALZ003, 5VLL140BN9,
Rosolutamide (INNTooltip International Nonproprietary Name; developmental code name ASC-JM17, JM17, ALZ-003) is an agonist of nuclear respiratory factor 1 (NRF1), a nonsteroidal antiandrogen, and an androgen receptor degrader related to curcumin.[1][2][3][4][5] Other analogues like dimethylcurcumin (ASC-J9) are also known.[2][6]
3-hydroxy imidacloprid is an imidacloprid. It has a role as a neonicotinoid insectide and a nicotinic acetylcholine receptor agonist.
REF
- Ferroptosis-related small-molecule compounds in cancer therapy: Strategies and applicationsPublication Name: European Journal of Medicinal ChemistryPublication Date: 2022-12-15PMID: 36332549DOI: 10.1016/j.ejmech.2022.114861
- A small-molecule Nrf1 and Nrf2 activator mitigates polyglutamine toxicity in spinal and bulbar muscular atrophyPublication Name: Human Molecular GeneticsPublication Date: 2016-03-08PMCID: PMC5062587PMID: 26962150DOI: 10.1093/hmg/ddw073
SYN
SYN
SYN
COMPD B
SYN
SYN
PAT
Publication Number: EP-2104659-B1
Priority Date: 2007-01-08
Grant Date: 2015-07-29
- Compounds with (1e, 6e)-1,7-bis-(3,4-dimethoxyphenyl)-4-4-disubstituted-hepta-1,6-diene-3,5-dione structural scaffold, their biological activity, and uses thereofPublication Number: US-2016264539-A1Priority Date: 2007-01-08
- Compounds with (substituted phenyl)-propenal moiety, their derivatives, biological activity, and uses thereofPublication Number: DK-2104659-T3Priority Date: 2007-01-08Grant Date: 2015-11-02
- Compounds with (1E, 6E)-1,7-Bis-(3,4-dimethoxyphenyl)-4-4-distributed-hepta-1,6-diene-3,5-dione structural scaffold, their biological activity, and uses thereofPublication Number: US-9562025-B2Priority Date: 2007-01-08Grant Date: 2017-02-07
- Compounds with (1E, 6E)-1,7-bis-(3,4-dimethoxyphenyl)-4,4-disubstituted-hepta-1,6-diene-3,5-dione structural scaffold, their biological activity, and uses thereofPublication Number: US-9000222-B2Priority Date: 2007-01-08Grant Date: 2015-04-07
- Compounds with (1 E, 6E)-1,7-bis-(3,4-dimethoxyphenyI)-4,4-disubstituted-hepta-1,6-diene-3,5-dione structural scaffold, their biological activity, and uses thereofPublication Number: US-9259402-B2Priority Date: 2007-01-08Grant Date: 2016-02-16
- Compounds with (1 E, 6E)-1,7-bis-(3,4-dimethoxyphenyl)-4,4-disubstituted-hepta-1,6-diene-3,5-dione structural scaffold, their biological activity, and uses thereofPublication Number: US-8710272-B2Priority Date: 2007-01-08Grant Date: 2014-04-29
- Compounds with (substituted phenyl)-propenal moiety, their derivatives, biological activity, and use thereofPublication Number: EP-2993165-A2Priority Date: 2007-01-08
- Compounds with (substituted phenyl)-propenal moiety, their derivatives, biological activity, and use thereofPublication Number: EP-2993165-B1Priority Date: 2007-01-08Grant Date: 2018-06-27
- Compounds with (1E, 6E)-1,7-bis-(3,4-dimethoxyphenyl)-4,4-disubstituted-hepta-1,6-diene-3,5-dione structural scaffold, their biological activity, and uses thereofPublication Number: US-2013261121-A1Priority Date: 2007-01-08
- Compounds with (substituted phenyl)-propenal moiety, their derivatives, biological activity, and uses thereofPublication Number: CA-2674780-CPriority Date: 2007-01-08Grant Date: 2014-03-11
- Compositions including androgen receptor degradation (ard) enhancers and methods of prophylactic or therapeutic treatment of skin disorders and hair lossPublication Number: CA-2694953-CPriority Date: 2007-07-31Grant Date: 2015-12-01
- Compositions containing androgen receptor degradation enhancers and methods for preventing or treating hair loss and skin diseasesPublication Number: KR-20100051808-APriority Date: 2007-07-31
- Compositions containing androgen receptor degradation (ARD) enhancers and methods for the prophylactic or therapeutic treatment of skin diseases and hair lossPublication Number: JP-2010535213-APriority Date: 2007-07-31
- Compounds with (1E, 6E)-1,7-bis-(3,4-dimethoxyphenyl)-4,4-disubstituted-hepta-1,6-diene-3,5-dione structural scaffold, their biological activity, and uses thereofPublication Number: US-2013338160-A1Priority Date: 2007-01-08
- Compounds with (1E, 6E)-1,7-bis-(3,4-dimethoxyphenyl)-4,4-disubstituted-hepta-1,6-diene-3,5-dione structural scaffold, their biological activity, and uses thereofPublication Number: US-2015190351-A1Priority Date: 2007-01-08
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| Clinical data | |
|---|---|
| Other names | ASC-JM-17; ASC-JM17; JM17; ALZ-003; ALZ003 |
| Identifiers | |
| IUPAC name | |
| CAS Number | 1039760-91-2 |
| PubChem CID | 25183127 |
| DrugBank | DB16931 |
| ChemSpider | 64854816 |
| UNII | 5VLL140BN9 |
| ChEMBL | ChEMBL5266600 |
| Chemical and physical data | |
| Formula | C28H32O6 |
| Molar mass | 464.558 g·mol−1 |
| 3D model (JSmol) | Interactive image |
| SMILES | |
| InChI | |
References
- “Proposed INN: List 131 International Nonproprietary Names for Pharmaceutical Substances (INN)” (PDF). WHO Drug Information. 38 (2): 428. 2024.
- Chang KH, Chen CM (May 2024). “The Role of NRF2 in Trinucleotide Repeat Expansion Disorders”. Antioxidants. 13 (6): 649. doi:10.3390/antiox13060649. PMC 11200942. PMID 38929088.
- Yuan J, Zhang S, Zhang Y (December 2018). “Nrf1 is paved as a new strategic avenue to prevent and treat cancer, neurodegenerative and other diseases”. Toxicology and Applied Pharmacology. 360: 273–283. Bibcode:2018ToxAP.360..273Y. doi:10.1016/j.taap.2018.09.037. PMID 30267745.
- Bott LC, Badders NM, Chen KL, Harmison GG, Bautista E, Shih CC, et al. (May 2016). “A small-molecule Nrf1 and Nrf2 activator mitigates polyglutamine toxicity in spinal and bulbar muscular atrophy”. Human Molecular Genetics. 25 (10): 1979–1989. doi:10.1093/hmg/ddw073. PMC 5062587. PMID 26962150.
- Wu YL, Chang JC, Chao YC, Chan H, Hsieh M, Liu CS (July 2022). “In Vitro Efficacy and Molecular Mechanism of Curcumin Analog in Pathological Regulation of Spinocerebellar Ataxia Type 3”. Antioxidants. 11 (7): 1389. doi:10.3390/antiox11071389. PMC 9311745. PMID 35883884.
- Sangotra A, Lieberman AP (February 2025). “Therapeutic targeting of the polyglutamine androgen receptor in Spinal and Bulbar Muscular Atrophy”. Expert Opinion on Therapeutic Targets: 1–13. doi:10.1080/14728222.2025.2464173. PMID 39915972.
/////////rosolutamide, antiandrogen, ASC-JM-17, ASC-JM17, JM17, ALZ-003, ALZ003, 5VLL140BN9, ANAX
Gridegalutamide
Gridegalutamide
CAS 2446929-86-6
MF C41H45F3N8O5S MW818.9 g/mol
2-[(2R)-4-[2-[4-[3-[4-cyano-3-(trifluoromethyl)phenyl]-5,5-dimethyl-4-oxo-2-sulfanylideneimidazolidin-1-yl]-2-ethylphenoxy]ethyl]-2-methylpiperazin-1-yl]-N-[3-[[(3R)-2,6-dioxopiperidin-3-yl]amino]phenyl]acetamide
antiandrogen, antineoplastic, BMS 986365, CC 94676, BMS-986365, CC-94676, CEL 010355,
VA228VR2DI,
Gridegalutamide is an investigational oral androgen receptor (AR) degrader being developed for the treatment of metastatic castration-resistant prostate cancer (mCRPC). It belongs to a class of drugs called proteolysis targeting chimeras (PROTACs), which are designed to selectively degrade specific proteins by hijacking the ubiquitin-proteasome system.[1][2] CC-94676 employs a unique dual mechanism of action, combining AR degradation with AR antagonism, potentially offering advantages over traditional AR inhibitors in overcoming resistance mechanisms.[3] Initially developed by Celgene and now under Bristol Myers Squibb, CC-94676 has demonstrated AR protein degradation and suppression of tumor growth in CRPC mouse models.[2] As of 2024, CC-94676 is being evaluated in phase I clinical trials for patients with mCRPC who have progressed on androgen deprivation therapy and at least one prior secondary hormonal therapy.[1][2]
Gridegalutamide is a small molecule drug. The usage of the INN stem ‘-lutamide’ in the name indicates that Gridegalutamide is a non-steroid antiandrogen. Gridegalutamide is under investigation in clinical trial NCT04428788 (Study to Evaluate the Safety and Tolerability of CC-94676 in Participants With Metastatic Castration-Resistant Prostate Cancer). Gridegalutamide has a monoisotopic molecular weight of 818.32 Da.
GRIDEGALUTAMIDE is a small molecule drug with a maximum clinical trial phase of II (across all indications) and has 3 investigational indications.
Gridegalutamide is an orally bioavailable androgen receptor (AR) degrader, with potential antineoplastic activity. Upon administration, gridegalutamide causes degradation of AR, prevents AR-mediated signaling and inhibits the proliferation of AR-overexpressing tumor cells. AR plays a key role in tumor cell proliferation in castration-resistant prostate cancer (CRPC).
- A Study to Evaluate the Drug Levels, Metabolism and Excretion, and Absolute Bioavailability of BMS-986365 in Healthy Male ParticipantsCTID: NCT06433505Phase: Phase 1Status: CompletedDate: 2025-03-26
- Study to Evaluate the Safety and Tolerability of CC-94676 in Participants With Metastatic Castration-Resistant Prostate CancerCTID: NCT04428788Phase: Phase 1Status: CompletedDate: 2025-12-22
SYN
DRUGHUNTER
https://drughunter.com/molecule/gridegalutamide-bms-986365-cc-94676
PAT
Example 17: 2-((R)-4-(2-(4-(3-(4-Cyano-3-(trifluoromethyl)phenyl)-5,5-dimethyl-4-oxo-2- thioxoimidazolidin-1-yl)-2-ethylphenoxy)ethyl)-2-methylpiperazin-1-yl)-N-(3-((2,6- dioxopiperidin-3-yl)amino)phenyl)acetamide hydrochloride
PAT
- Combination therapy with substituted 3- ((3-aminophenyl) amino) piperidine-2, 6-dione compoundsPublication Number: CN-120152718-APriority Date: 2022-11-09
- Combination therapy with substituted 3-((3-aminophenyl)amino)piperidine-2,6-dione compoundsPublication Number: WO-2024102706-A1Priority Date: 2022-11-09
- Substituted 3-((3-aminophenyl)amino)piperidine-2,6-dione compounds, compositions thereof, and methods of treatment therewithPublication Number: US-2020199073-A1Priority Date: 2018-12-19
- Substituted 3-((3-aminophenyl)amino)piperidine-2,6-dione compounds, compositions thereof, and methods of treatment therewithPublication Number: US-11149007-B2Priority Date: 2018-12-19Grant Date: 2021-10-19
- Substituted 3-((3-aminophenyl)amino)piperidine-2,6-dione compounds, compositions thereof, and methods of treatment therewithPublication Number: US-11873283-B2Priority Date: 2018-12-19Grant Date: 2024-01-16
- Substituted 3-((3-aminophenyl)amino)piperidine-2,6-dione compounds, compositions thereof, and methods of treatment therewithPublication Number: US-2024368083-A1Priority Date: 2018-12-19
- Substituted 3-((3-aminophenyl)amino)piperidine-2,6-dione compounds, compositions thereof, and methods of treatment therewithPublication Number: US-12404241-B2Priority Date: 2018-12-19Grant Date: 2025-09-02
- Substituted 3-((3-aminophenyl)amino)piperidine-2,6-dione compounds, compositions thereof, and methods of treatment therewithPublication Number: US-2023002321-A1Priority Date: 2018-12-19
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References
- Salama AK, Trkulja MV, Casanova E, Uras IZ (December 2022). “Targeted Protein Degradation: Clinical Advances in the Field of Oncology”. International Journal of Molecular Sciences. 23 (23) 15440. doi:10.3390/ijms232315440. PMC 9741350. PMID 36499765.
- Xie H, Liu J, Alem Glison DM, Fleming JB (2021). “The clinical advances of proteolysis targeting chimeras in oncology”. Exploration of Targeted Anti-Tumor Therapy. 2 (6): 511–521. doi:10.37349/etat.2021.00061. PMC 9400722. PMID 36046114.
- Rathkopf DE, Patel MR, Choudhury AD, Rasco D, Lakhani N, Hawley JE, et al. (September 2024). “Safety and clinical activity of BMS-986365 (CC-94676), a dual androgen receptor ligand-directed degrader and antagonist, in heavily pretreated patients with metastatic castration-resistant prostate cancer”. Annals of Oncology. 36 (1): 76–88. doi:10.1016/j.annonc.2024.09.005. PMC 12094577. PMID 39293515.
| Clinical data | |
|---|---|
| Other names | BMS-986365; CC-94676 |
| Identifiers | |
| IUPAC name | |
| CAS Number | 2446929-86-6 |
| PubChem CID | 153513643 |
| ChemSpider | 133326102 |
| UNII | VA228VR2DI |
| KEGG | D12866 |
| ChEMBL | ChEMBL6068413 |
| Chemical and physical data | |
| Formula | C41H45F3N8O5S |
| Molar mass | 818.92 g·mol−1 |
| 3D model (JSmol) | Interactive image |
| SMILES | |
| InChI | |
//////////gridegalutamide, ANAX, ADVECT, antiandrogen, antineoplastic, BMS 986365, CC 94676, BMS-986365, CC-94676, CEL 010355, VA228VR2DI,
New Drug Approvals 
