# US 8,772,325 B2 · Compounds as opioid receptor modulators > Agents: this data is available as JSON from the patentgrep API and MCP server — see https://patentgrep.com/llms.txt - Number: US 8,772,325 B2 - Document ID: US8772325B2 - Status: Granted - Kind: B2 - Application number: 14/045,008 - Filed: 2013-10-03 - Published: 2014-02-06 - Granted: 2014-07-08 - Earliest claimed: 2004-03-15 - Assignees: Janssen Pharmaceutica NV - Applicants: Jannsen Pharmaceutica, N.V. - Inventors: Henry J. Breslin; Chaozhong Cai; Wei He; Robert W. Kavash - Web page: https://patentgrep.com/patent/US8772325B2 ## CPC - A61K 31/4164: 1,3-Diazoles - A61K 9/20: Pills, tablets, {discs, rods (A61K9/0004, A61K9/0007, A61K9/0056, A61K9/0065 take precedence; for reconstitution of a drink A61K9/0095)} - A61K 9/2806: {Coating materials} - A61K 31/4174: Arylalkylimidazoles, e.g. oxymetazolin, naphazoline, miconazole - A61P 1/00: Drugs for disorders of the alimentary tract or the digestive system - A61P 1/04: for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants - A61P 1/10: Laxatives - A61P 1/12: Antidiarrhoeals - A61P 25/00: Drugs for disorders of the nervous system - A61P 25/02: for peripheral neuropathies - A61P 25/04: Centrally acting analgesics, e.g. opioids - A61P 25/06: Antimigraine agents - A61P 29/00: Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID] - C07D 233/64: with substituted hydrocarbon radicals attached to ring carbon atoms, e.g. histidine - C07D 275/06: with hetero atoms directly attached to the ring sulfur atom - A61K: PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES (devices or methods specially adapted for bringing pharmaceutical products into particular physical or administering forms A61J3/00; chemical aspects of, or use of materials for deodorisation of air, for disinfection or sterilisation, or for bandages, dressings, absorbent pads or surgical articles A61L; soap compositions C11D) - A61P: SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS - C07D: HETEROCYCLIC COMPOUNDS (macromolecular compounds C08) ## Abstract The present invention is directed to novel opioid receptor modulators of Formula (I). The invention further relates to methods for preparing such compounds, pharmaceutical compositions containing them, and their use in the treatment of disorders that may be ameliorated or treated by the modulation of opioid receptors. ## Claims ### Claim 1 A method for treating pain or gastrointestinal disorder, wherein said pain is centrally mediated pain, peripherally mediated pain, structural or soft tissue injury related pain, pain related to inflammation, progressive disease related pain, neuropathic pain, acute pain, or chronic pain, and wherein said gastrointestinal disorder is ulcerative colitis, Crohn's disease, diarrhea-predominant irritable bowel syndrome, or alternating irritable bowel syndrome, in a subject in need thereof comprising administering to the subject a therapeutically effective amount of a compound having the structure: or a pharmaceutically acceptable salt thereof. ### Claim 2 (depends on 1) The method according to claim 1, wherein said compound has the structure: ### Claim 3 (depends on 2) The method according to claim 2, wherein said compound has the structure: ### Claim 4 (depends on 2) The method according to claim 2, wherein said compound has the structure: ### Claim 5 (depends on 2) The method according to claim 2, wherein said compound has the structure: ### Claim 6 (depends on 1) The method according to claim 1, comprising administering to the subject a therapeutically effective amount of a pharmaceutically acceptable salt of said compound. ### Claim 7 (depends on 6) The method according to claim 6, wherein the salt is a hydrochloric, hydrobromic, hydriodic, perchloric, sulfuric, nitric, phosphoric, acetic, propionic, glycolic, lactic, succinic, maleic, fumaric, malic, tartaric, citric, benzoic, mandelic, methanesulfonic, hydroxyethanesulfonic, benzenesulfonic, oxalic, pamoic, 2-naphthalenesulfonic, p-toluenesulfonic, cyclohexanesulfamic, salicylic, saccharinic, or trifluoroacetic acid salt. ### Claim 8 (depends on 6) The method according to claim 6, wherein the salt is a benzathine, chloroprocaine, choline, diethanolamine, ethylenediamine, meglumine, procaine, aluminum, calcium, lithium, magnesium, potassium, sodium, or zinc salt. ### Claim 9 (depends on 1) The method according to claim 1, wherein the chronic pain is selected from the group consisting of neuropathic pain conditions, diabetic peripheral neuropathy, post-herpetic neuralgia, trigeminal neuralgia, post-stroke pain syndromes and cluster or migraine headaches. ### Claim 10 (depends on 1) The method of claim 1, wherein the method is for treating centrally mediated pain. ### Claim 11 (depends on 1) The method according to claim 1, wherein the method is for treating peripherally mediated pain. ### Claim 12 (depends on 1) The method according to claim 1, wherein the method is for treating structural or soft tissue injury related pain. ### Claim 13 (depends on 1) The method according to claim 1, wherein the method is for treating pain related to inflammation. ### Claim 14 (depends on 1) The method according to claim 1, wherein the method is for treating progressive disease related pain. ### Claim 15 (depends on 1) The method according to claim 1, wherein the method is for treating neuropathic pain. ### Claim 16 (depends on 1) The method according to claim 1, wherein the method is for treating acute pain. ### Claim 17 (depends on 1) The method according to claim 1, wherein the method is for treating chronic pain. ### Claim 18 (depends on 17) The method according to claim 17, wherein the chronic pain is selected from the group consisting of neuropathic pain conditions, diabetic peripheral neuropathy, post-herpetic neuralgia, trigeminal neuralgia, post-stroke pain syndromes and cluster or migraine headaches. ### Claim 19 (depends on 1) The method according to claim 1, wherein the method is for treating ulcerative colitis. ### Claim 20 (depends on 1) The method according to claim 1, wherein the method is for treating Crohn's disease. ### Claim 21 (depends on 1) The method according to claim 1, wherein the method is for treating diarrhea-predominant irritable bowel syndrome. ### Claim 22 (depends on 1) The method according to claim 1, wherein the method is for treating alternating irritable bowel syndrome. ### Claim 23 A method for treating diarrhea-predominant irritable bowel syndrome in a subject in need thereof comprising administering to the subject a therapeutically effective amount of a compound having the structure: or a pharmaceutically acceptable salt thereof.