Fosaprepitant

Fosaprepitant

SCHEMBL156378

CNC[C@H](O)[C@@H](O)[C@H](O)[C@H](O)CO.C[C@@H](OC1OCCN(Cc2nc(=O)n(P(=O)(O)O)[nH]2)C1c1ccc(F)cc1)c1cc(C(F)(F)F)cc(C(F)(F)F)c1

nearest known ligand 0.59

Full drug profile on Sugi Atlas →

Known targets — ChEMBL curated mechanism

TACR1

The experimentally established mechanism targets of Fosaprepitant. 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 0.59
TACR3 P29371 2/20 0.59
NR3C1 P04150 1/20 0.59
CYP3A4 P08684 1/20 0.59
FPR1 P21462 1/20 0.59
GPR183 P32249 1/20 0.59
OPRD1 P41143 1/20 0.59
GPR65 Q8IYL9 1/20 0.59
GPR35 Q9HC97 1/20 0.59
TACR2 P21452 1/20 0.38

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
Fosaprepitant SCHEMBL17837327 1.00 TACR1 (0.59) TACR1TACR3NR3C1CYP3A4FPR1
Fosaprepitant SCHEMBL22076807 1.00 TACR1 (0.59) TACR1TACR3NR3C1CYP3A4FPR1
Fosaprepitant SCHEMBL30861885 1.00 TACR1 (0.59) TACR1TACR3NR3C1CYP3A4FPR1
SCHEMBL1932400 0.92 TACR1 (0.57) TACR1TACR3NR3C1CYP3A4FPR1
Fosaprepitant SCHEMBL21955651 0.91 TACR1 (0.71) TACR1TACR3NR3C1CYP3A4FPR1
Fosaprepitant SCHEMBL1651366 0.91 TACR1 (0.71) TACR1TACR3NR3C1CYP3A4FPR1
SCHEMBL20473749 0.90 TACR1 (0.60) TACR1TACR3NR3C1CYP3A4FPR1
SCHEMBL21391935 0.89 TACR1 (0.57) TACR1TACR3NR3C1CYP3A4FPR1
SCHEMBL22076806 0.89 TACR1 (0.59) TACR1TACR3NR3C1CYP3A4FPR1
SCHEMBL156379 0.89 TACR1 (0.59) 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 83 patents — showing the first 20. claimed = in the patent's claims; disclosed = body only.

PatentTitleAssigneePublishedPriorityFilingCountryStatus
US-20220008400-A1 METHODS OF TREATING AUTOIMMUNE, RESPIRATORY AND INFLAMMATORY DISORDERS BY INHALATION OF ROFLUMILAST N-OXIDE INCOZEN THERAPEUTICS PVT LTD (IN) 2022-01-13 US disclosed
EP-3763366-A1 ROFLUMILAST N-OXIDE FOR USE IN TREATING AUTOIMMUNE, RESPIRATORY AND INFLAMMATORY DISORDERS BY INHALATION Incozen Therapeutics Pvt. Ltd. (IN) 2021-01-13 EP disclosed
EP-2948148-B1 METHODS OF TREATING AUTOIMMUNE, RESPIRATORY AND INFLAMMATORY DISORDERS BY INHALATION OF ROFLUMILAST N-OXIDE INCOZEN THERAPEUTICS PVT LTD (IN) 2020-07-29 EP disclosed
EP-3024459-B1 COMBINATIONS COMPRISING MABA COMPOUNDS AND CORTICOSTEROIDS ALMIRALL SA (ES) 2019-03-27 EP disclosed
US-20180200234-A1 COMBINATIONS COMPRISING ANTIMUSCARINIC AGENTS AND BETA-ADRENERGIC AGONISTS ALMIRALL, S.A. (ES) 2018-07-19 US disclosed
US-20170196843-A1 METHODS OF TREATING AUTOIMMUNE, RESPIRATORY AND INFLAMMATORY DISORDERS BY INHALATION OF ROFLUMILAST N-OXIDE INCOZEN THERAPEUTICS PVT LTD (IN) 2017-07-13 US disclosed
US-9649302-B2 Methods of treating autoimmune, respiratory and inflammatory disorders by inhalation of roflumilast N-oxide INCOZEN THERAPEUTICS PVT. LTD. (IN) 2017-05-16 US disclosed
US-20160038470-A1 COMBINATIONS COMPRISING ANTIMUSCARINIC AGENTS AND CORTICOSTEROIDS GRAS ESCARDO JORDI (ES) 2016-02-11 US disclosed
US-20160015704-A1 COMBINATIONS COMPRISING MABA COMPOUNDS AND CORTICOSTEROIDS ALMIRALL, S.A. (ES) 2016-01-21 US disclosed
US-20150306079-A1 COMBINATIONS COMPRISING ANTIMUSCARINIC AGENTS AND PDE4 INHIBITORS GRAS ESCARDO JORDI (ES) 2015-10-29 US disclosed
EP-1891973-A1 Combinations comprising antimuscarinic agents and PDE4 inhibitors Laboratorios Almirall, S.A. (ES) 2008-02-27 EP disclosed
US-20080045565-A1 Combinations Comprising Antimuscarinic Agents and Beta-Adrenergic Agonists LABORATORIOS ALMIRALL, S.A. (ES) 2008-02-21 US disclosed
US-20070232637-A1 Combinations Comprising Antimuscarinic Agents and Pde4 Inhibitors LABORATORIOS ALMIRALL, S.A. (ES) 2007-10-04 US disclosed
US-20070167489-A1 Combination comprising antimuscarinic agents and PDE4 inhibitors GRAS ESCARDO JORDI 2007-07-19 US disclosed
US-20060205702-A1 Combinations comprising antimuscarinic agents and corticosteroids LABORATORIOS ALMIRALL, S.A. (ES) 2006-09-14 US disclosed
US-20060189651-A1 Combinations comprising antimuscarinic agents and beta-adrenergic agonists LABORATORIOS ALMIRALL, S.A. (ES) 2006-08-24 US disclosed
US-20060154934-A1 Combinations comprising antimuscarinic agents and PDE4 inhibitors LABORATORIOS ALMIRALL, S.A. (ES) 2006-07-13 US disclosed
US-20050288266-A1 Combinations comprising antimuscarinic agents and corticosteroids GRAS ESCARDO JORDI 2005-12-29 US disclosed
US-20050267135-A1 Combinations comprising antimuscarinic agents and PDE4 inhibitors ESCARDO JORDI G 2005-12-01 US disclosed
US-20050267078-A1 Combinations comprising antimuscarinic agents and beta-adrenergic agonists GRAS ESCARDO JORDI 2005-12-01 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 (15 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-20220008400-A1 METHODS OF TREATING AUTOIMMUNE, RESPIRATORY AND INFLAMMATORY DISORDERS BY INHALATION OF ROFLUMILAST N-OXIDE NOS3, NOS2, NOS1 TACR1 1131/4885TACR3 1848/4885NR3C1 885/4885
US-20060189651-A1 Combinations comprising antimuscarinic agents and beta-adrenergic agonists ADRB2, ADRB3, CHRM3 TACR1 72/4885TACR3 117/4885NR3C1 282/4885
US-20080045565-A1 Combinations Comprising Antimuscarinic Agents and Beta-Adrenergic Agonists CHRM3, ADRB2, CHRM2 TACR1 78/4885TACR3 142/4885NR3C1 626/4885
US-20180200234-A1 COMBINATIONS COMPRISING ANTIMUSCARINIC AGENTS AND BETA-ADRENERGIC AGONISTS ADRB2, ADRB3, CHRM3 TACR1 72/4885TACR3 117/4885NR3C1 282/4885
US-20050267135-A1 Combinations comprising antimuscarinic agents and PDE4 inhibitors CHRM3, PDE4A, CHRM4 TACR1 141/4885TACR3 213/4885NR3C1 591/4885
US-20050267078-A1 Combinations comprising antimuscarinic agents and beta-adrenergic agonists ADRB2, ADRB3, CHRM3 TACR1 72/4885TACR3 117/4885NR3C1 282/4885
US-20070167489-A1 Combination comprising antimuscarinic agents and PDE4 inhibitors CHRM3, PDE4A, CHRM4 TACR1 141/4885TACR3 215/4885NR3C1 596/4885
US-20150306079-A1 COMBINATIONS COMPRISING ANTIMUSCARINIC AGENTS AND PDE4 INHIBITORS CHRM3, PDE4A, CHRM4 TACR1 156/4885TACR3 182/4885NR3C1 642/4885
US-20160015704-A1 COMBINATIONS COMPRISING MABA COMPOUNDS AND CORTICOSTEROIDS ADRB2, ADRA2A, ADRA2B TACR1 810/4885TACR3 641/4885NR3C1 15/4885
US-20170196843-A1 METHODS OF TREATING AUTOIMMUNE, RESPIRATORY AND INFLAMMATORY DISORDERS BY INHALATION OF ROFLUMILAST N-OXIDE NOS3, NOS2, NOS1 TACR1 1131/4885TACR3 1848/4885NR3C1 885/4885
US-20060154934-A1 Combinations comprising antimuscarinic agents and PDE4 inhibitors CHRM3, PDE4A, CHRM4 TACR1 141/4885TACR3 213/4885NR3C1 591/4885
US-20060205702-A1 Combinations comprising antimuscarinic agents and corticosteroids CHRM3, CHRM2, CHRM1 TACR1 67/4885TACR3 153/4885NR3C1 18/4885
US-20070232637-A1 Combinations Comprising Antimuscarinic Agents and Pde4 Inhibitors CHRM3, CHRM4, PDE4A TACR1 121/4885TACR3 125/4885NR3C1 1509/4885
US-20160038470-A1 COMBINATIONS COMPRISING ANTIMUSCARINIC AGENTS AND CORTICOSTEROIDS CHRM3, CHRM2, CHRM1 TACR1 67/4885TACR3 153/4885NR3C1 18/4885
US-20050288266-A1 Combinations comprising antimuscarinic agents and corticosteroids CHRM3, CHRM2, CHRM1 TACR1 67/4885TACR3 153/4885NR3C1 18/4885

“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.