Asimadoline

Asimadoline

SCHEMBL1179586

CN(C(=O)C(c1ccccc1)c1ccccc1)[C@H](CN1CC[C@H](O)C1)c1ccccc1.Cl

nearest known ligand 1.00 ✓ in ChEMBL — recovers established targets

Full drug profile on Sugi Atlas →

Known targets — ChEMBL curated mechanism

OPRK1

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

Predicted protein targets (top 4)

geneUniProtsupporting neighboursconfidence
OPRK1 known ✓ P41145 3/20 0.98
OPRM1 P35372 1/20 0.98
OPRD1 P41143 1/20 0.98
CYP2D6 P10635 2/20 0.68

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
Asimadoline SCHEMBL8011656 1.00 OPRK1 (0.98) OPRK1OPRM1OPRD1CYP2D6
Asimadoline SCHEMBL26923202 1.00 OPRK1 (0.98) OPRK1OPRM1OPRD1CYP2D6
Asimadoline SCHEMBL7721982 0.99 OPRK1 (1.00) OPRK1OPRM1OPRD1CYP2D6
Asimadoline SCHEMBL6923822 0.99 OPRK1 (1.00) OPRK1OPRM1OPRD1CYP2D6
Asimadoline SCHEMBL8717354 0.99 OPRK1 (1.00) OPRK1OPRM1OPRD1CYP2D6
Asimadoline SCHEMBL155020 0.99 OPRK1 (1.00) OPRK1OPRM1OPRD1CYP2D6
Asimadoline SCHEMBL13639176 0.99 OPRK1 (1.00) OPRK1OPRM1OPRD1CYP2D6
Asimadoline SCHEMBL2473545 0.99 OPRK1 (1.00) OPRK1OPRM1OPRD1CYP2D6
SCHEMBL8720266 0.93 OPRK1 (0.89) OPRK1OPRM1OPRD1CYP2D6
SCHEMBL9015325 0.93 OPRK1 (0.89) OPRK1OPRM1OPRD1CYP2D6

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

PatentTitleAssigneePublishedPriorityFilingCountryStatus
US-8877800-B2 Kappa-opiate agonists for the treatment of diarrhea-predominant irritable bowel syndrome TIOGA PHARMACEUTICALS, INC. (US) 2014-11-04 US claimed
EP-2636407-A2 Kappa-opiate agonists for the treatment of diarrhea-predominant and alternating irritable bowel syndrome Tioga Pharmaceuticals, Inc. (US) 2013-09-11 EP claimed
EP-2561870-A1 Kappa-Opiate Agonists For The Treatment Of Diarrhea-Predominant and Alternating Irritable Bowel Syndrome Tioga Pharmaceuticals, Inc. (US) 2013-02-27 EP claimed
EP-2136801-B1 KAPPA-OPIATE AGONISTS FOR THE TREATMENT OF DIARRHEA-PREDOMINANT AND ALTERNATING IRRITABLE BOWEL SYNDROME TIOGA PHARMACEUTICALS INC (US) 2012-08-29 EP claimed
CN-102641265-A Kappa-opiate agonists for the treatment of diarrhea-predominant and alternating irritable bowel syndrome TIOGA PHARMACEUTICALS INC 2012-08-22 CN claimed
CN-101677997-B Kappa-opiate agonists for the treatment of diarrhea-predominant and alternating irritable bowel syndrome TIOGA PHARMACEUTICALS INC 2012-05-09 CN claimed
US-7960429-B2 especially N-methyl-N-[(1S)-1-phenyl-2-((3S)-3-hydroxypyrrolidin-1-yl)ethyl]-2,2-diphenylacetamide (Asimadoline) or salt; reduces symptoms of abnormal stool frequency, abnormal stool form, defecation straining, urgency, a feeling of incomplete bowel movement, passing mucus, and bloating Tioga Pharmaceuticals, Inc (US) 2011-06-14 US claimed
US-20110046174-A1 KAPPA-OPIATE AGONISTS FOR THE TREATMENT OF DIARRHEA-PREDOMINANT IRRITABLE BOWEL SYNDROME TIOGA PHARMACEUTICALS, INC. (US) 2011-02-24 US claimed
CN-101677997-A Kappa-opiate agonists for the treatment of diarrhea-predominant and alternating irritable bowel syndrome TIOGA PHARMACEUTICALS INC 2010-03-24 CN claimed
EP-2074997-A1 Use of Asimadoline for the treatment of digestive disorders Tioga Pharmaceuticals, Inc. (US) 2009-07-01 EP claimed
US-20070179098-A1 Treatment of functional dyspepsia using asimadoline MERCK PATENT GESELLSCHAFT MIT BESCHRANKTER HAFTUNG (DE) 2007-08-02 US claimed
US-20010051181-A1 NOVEL FORMULATIONS FOR THE TRANSDERMAL ADMINISTRATION OF ASIMADOLINE VAN OSDOL WILLIAM W (US) 2001-12-13 US claimed
EP-0761650-B1 Thermally stable and storable crystalline modification of N-methyl-N-((1S)-1-phenyl-2-((3S)-3-hydroxypyrrolidin-1-yl)-ethyl)-2,2-diphenyl-acetamide and process for its preparation MERCK PATENT GMBH (DE) 2001-10-31 EP claimed
US-6060504-A N-methyl-N-[(1S)-1-phenyl-2-(3S)-hydroxypyrrolidin-1-yl)ethyl]-2-2-diphenylacetamide MERCK PATENT GESELLSCHAFT MIT BESCHRANKTER HAFTUNG (DE) 2000-05-09 US claimed
US-5977161-A Administering asimadoline hydrochloride MERCK PATENT GESELLSCHAFT MIT BESCHRANKTER HAFTUNG (DE) 1999-11-02 US claimed
WO-1999032096-A1 NOVEL FORMULATIONS FOR THE TRANSDERMAL ADMINISTRATION OF ASIMADOLINE ALZA CORPORATION (US) 1999-07-01 WO claimed
US-5776972-A USE OF ASIMADOLINE HYDROCHLORIDE (N-methyl-N-((1S)-1-phenyl-2-((3S)-3-hydRoxypyrrolidin-1-yl)-ethyl)-2,2-diphenyl-acetamide hydrochloride) MERCK PATENT GESELLSCHAFT MIT BESCHRANKTER HAFTUNG (DE) 1998-07-07 US claimed
CN-1145781-A Kappa-opiate agonists for inflammatory bowel disorders MERCK PATENT GMBH (DE) 1997-03-26 CN claimed
EP-0761650-A1 Thermally stable and storable crystalline modification of N-methyl-N-((1S)-1-phenyl-2-((3S)-3-hydroxypyrrolidin-1-yl)-ethyl)-2,2-diphenyl-acetamide and process for its preparation MERCK PATENT GmbH (DE) 1997-03-12 EP claimed
EP-0752246-A2 Kappa opiate agonists for inflammatory gut diseases MERCK PATENT GmbH (DE) 1997-01-08 EP claimed

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

For each of this compound's patents that has machine-readable text (2 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-20110046174-A1 KAPPA-OPIATE AGONISTS FOR THE TREATMENT OF DIARRHEA-PREDOMINANT IRRITABLE BOWEL SYNDROME OPRD1, OPRK1, OPRL1 OPRK1 2/4885OPRM1 4/4885OPRD1 1/4885
US-20070179098-A1 Treatment of functional dyspepsia using asimadoline AADAC, CYP2A7, UGT2B7 OPRK1 252/4885OPRM1 82/4885OPRD1 38/4885

“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.