Aprepitant

Aprepitant

SCHEMBL1762934

CC(OC1OCCN(Cc2nc(=O)[nH][nH]2)C1c1ccc(F)cc1)c1cc(C(F)(F)F)cc(C(F)(F)F)c1

nearest known ligand 0.78

Full drug profile on Sugi Atlas →

Known targets — ChEMBL curated mechanism

TACR1

The experimentally established mechanism targets of Aprepitant. The predicted profile below is derived independently by chemical similarity — agreement is a validation signal, a miss is honest.

Predicted protein targets (top 10)

geneUniProtsupporting neighboursconfidence
TACR1 known ✓ P25103 18/20 0.78
TACR3 P29371 2/20 0.78
NR3C1 P04150 1/20 0.78
CYP3A4 P08684 1/20 0.78
FPR1 P21462 1/20 0.78
GPR183 P32249 1/20 0.78
OPRD1 P41143 1/20 0.78
GPR65 Q8IYL9 1/20 0.78
GPR35 Q9HC97 1/20 0.78
TACR2 P21452 1/20 0.49

Click a target to see other patent compounds predicted against it — the reverse direction, in place.

Similar compounds — the chemically nearest patent molecules

Nearest neighbours by Morgan-fingerprint cosine across the patent-compound collection, with each neighbour's top predicted target and the predicted targets it shares with this molecule.

Compoundsimilaritytop predictedshared targets
Aprepitant SCHEMBL28850 1.00 TACR1 (0.78) TACR1TACR3NR3C1CYP3A4FPR1
Aprepitant SCHEMBL264924 1.00 TACR1 (0.78) TACR1TACR3NR3C1CYP3A4FPR1
Aprepitant SCHEMBL16770383 1.00 TACR1 (0.78) TACR1TACR3NR3C1CYP3A4FPR1
Aprepitant SCHEMBL2687974 1.00 TACR1 (0.78) TACR1TACR3NR3C1CYP3A4FPR1
Aprepitant SCHEMBL1472775 1.00 TACR1 (0.78) TACR1TACR3NR3C1CYP3A4FPR1
Aprepitant SCHEMBL24067953 1.00 TACR1 (0.78) TACR1TACR3NR3C1CYP3A4FPR1
SCHEMBL17131462 0.97 TACR1 (0.74) TACR1TACR3NR3C1CYP3A4FPR1
SCHEMBL16768624 0.95 TACR1 (0.72) TACR1TACR3NR3C1CYP3A4FPR1
SCHEMBL5223102 0.89 TACR1 (0.62) TACR1TACR3NR3C1CYP3A4FPR1
SCHEMBL5223100 0.89 TACR1 (0.62) TACR1TACR3NR3C1CYP3A4FPR1

Similarity is cosine over the 2,048-bit Morgan fingerprint (≈ Tanimoto). Identical fingerprints score 1.00.

Patent provenance — the patents this molecule appears in, and who filed them

Claimed or disclosed in 29 patents — showing the first 20. claimed = in the patent's claims; disclosed = body only.

PatentTitleAssigneePublishedPriorityFilingCountryStatus
US-20230190740-A1 AN NK-1 RECEPTOR ANTAGONIST FOR TREATING A DISEASE SELECTING FROM SEPSIS, SEPTIC SHOCK, ACUTE RESPIRATORY DISTRESS SYNDROME (ARDS) OR MULTIPLE ORGAN DYSFUNCTION SYNDROME (MODS) NERRE THERAPEUTICS LIMITED (GB) 2023-06-22 US disclosed
US-20230190740-A1 AN NK-1 RECEPTOR ANTAGONIST FOR TREATING A DISEASE SELECTING FROM SEPSIS, SEPTIC SHOCK, ACUTE RESPIRATORY DISTRESS SYNDROME (ARDS) OR MULTIPLE ORGAN DYSFUNCTION SYNDROME (MODS) NERRE THERAPEUTICS LIMITED (GB) 2023-06-22 US disclosed
EP-4019023-A1 FORMULATIONS OF FOSAPREPITANT AND APREPITANT Zhuhai Beihai Biotech Co., Ltd. (CN) 2022-06-29 EP disclosed
EP-3493815-B1 FORMULATIONS OF FOSAPREPITANT AND APREPITANT ZHUHAI BEIHAI BIOTECH CO LTD (CN) 2022-02-16 EP disclosed
EP-2963019-B1 METHOD FOR PRODUCING PYRIDINE-3-SULFONYL CHLORIDE TAKEDA PHARMACEUTICALS CO (JP) 2020-08-12 EP disclosed
US-10370357-B2 Method for producing sulfonyl chloride compound TAKEDA PHARMACEUTICAL COMPANY LIMITED (JP) 2019-08-06 US disclosed
US-20180170905-A1 Method for Producing Sulfonyl Chloride Compound TAKEDA PHARMACEUTICAL COMPANY LIMITED (JP) 2018-06-21 US disclosed
EP-3305797-A1 ANTAGONISTS OF NK1 RECEPTORS DERIVED FROM CARBOHYDRATES, PRODUCTION METHOD AND MEDICAL USE Consejo Superior De Investigaciones Científicas (CSIC) (ES) 2018-04-11 EP disclosed
US-9932322-B2 Method for producing sulfonyl chloride compound TAKEDA PHARMACEUTICAL COMPANY LIMITED (JP) 2018-04-03 US disclosed
EP-2309985-B1 PHARMACEUTICAL COMPOSITION TAKEDA PHARMACEUTICALS CO (JP) 2018-03-14 EP disclosed
EP-2564833-A1 Photostabilized pharmaceutical composition Takeda Pharmaceutical Company Limited (JP) 2013-03-06 EP disclosed
CN-102939285-A Preparation method of 5-[[2(r)-[1(r)-[3,5-bis(trifluoromethyl)phenyl]ethoxy]-3(s)-4-fluorophenyl-4-morpholinyl]methyl]-1,2-dihydro-3h-1,2,4-triazole-3-one CHENGDU DI AO PHARMACEUTICAL GROUP CO LTD 2013-02-20 CN disclosed
CN-102939285-A Preparation method of 5-[[2(r)-[1(r)-[3,5-bis(trifluoromethyl)phenyl]ethoxy]-3(s)-4-fluorophenyl-4-morpholinyl]methyl]-1,2-dihydro-3h-1,2,4-triazole-3-one CHENGDU DI AO PHARMACEUTICAL GROUP CO LTD 2013-02-20 CN disclosed
US-8080656-B2 Process for the preparation of aprepitant RANBAXY LABORATORIES LIMITED (IN) 2011-12-20 US disclosed
US-20110124687-A1 PHARMACEUTICAL COMPOSITION TAKEDA PHARMACEUTICAL COMPANY LIMITED (JP) 2011-05-26 US disclosed
US-7718809-B2 Chromane substituted benzimidazole derivatives as acid pump antagonists RAQUALIA PHARMA INC. (JP) 2010-05-18 US disclosed
US-20100004242-A1 PROCESS FOR THE PREPARATION OF APREPITANT RANBAXY LABORATORIES LIMITED (IN) 2010-01-07 US disclosed
WO-2009124756-A1 USE OF APREPITANT AND DERIVATIVES THEREOF FOR THE TREATMENT OF CANCER EUROPEAN MOLECULAR BIOLOGY LABORATORY (EMBL) (DE) 2009-10-15 WO disclosed
WO-2008097546-A2 COMPOUNDS THAT INHIBIT CHOLINESTERASE COLUCID PHARMACEUTICALS, INC. (US) 2008-08-14 WO disclosed
US-20050215786-A1 reacting the hydrochloride salt of 1-[3,5-bis(trifluoromethyl)phenyl]ethoxy]-3-(4-fluorophenyl)morpholine with Methyl N-[(1-amino-2-chloro-ethylidene)amino]carbamate, in the presence of potassium carbonate, toluene and dimethylsulfoxide, then washing, drying, cyclization of the intermediate MERCK SHARP & DOHME LLC 2005-09-29 US disclosed

Patent text — is the patent's own abstract consistent with the prediction?

For each of this compound's patents that has machine-readable text (6 of them — usually the abstract, not the full specification), we ask MedCPT which protein the text reads most about, and where the chemistry-predicted target lands among 4885 human targets. A high rank means the patent's own wording is consistent with the prediction — a weak, independent signal, not proof of activity.

PatentTitleText reads most aboutPredicted target · text-rank
US-20110124687-A1 PHARMACEUTICAL COMPOSITION CYP2C19, MLST8, CYP3A43 TACR1 1303/4885TACR3 4129/4885NR3C1 2352/4885
US-10370357-B2 Method for producing sulfonyl chloride compound P2RY4, P2RY6, P2RX4 TACR1 54/4885TACR3 683/4885NR3C1 3321/4885
US-20230190740-A1 AN NK-1 RECEPTOR ANTAGONIST FOR TREATING A DISEASE SELECTING FROM SEPSIS, SEPTIC SHOCK, ACUTE RESPIRATORY DISTRESS SYNDROME (ARDS) OR MULTIPLE ORGAN DYSFUNCTION SYNDROME (MODS) KLKB1, KLK1, BDKRB1 TACR1 13/4885TACR3 58/4885NR3C1 224/4885
US-20100004242-A1 PROCESS FOR THE PREPARATION OF APREPITANT CMA1, CYP3A5, TPSB2 TACR1 16/4885TACR3 189/4885NR3C1 1776/4885
US-20050215786-A1 reacting the hydrochloride salt of 1-[3,5-bis(trifluoromethyl)phenyl]ethoxy]-3-(4-fluorophenyl)morpholine with Methyl N-[(1-amino-2-chloro-ethylidene)amino]carbamate, in the presence of potassium carbonate, toluene and dimethylsulfoxide, then washing, drying, cyclization of the intermediate TACR1, TACR2, NPSR1 TACR1 1/4885TACR3 4/4885NR3C1 217/4885
US-20180170905-A1 Method for Producing Sulfonyl Chloride Compound P2RY4, P2RY6, P2RX4 TACR1 54/4885TACR3 683/4885NR3C1 3321/4885

“Text reads most about” is the patent abstract's nearest protein in MedCPT space (background-debiased). Only ~1.4% of patents have machine-readable text, so most compounds won't have this panel.