IP Library › Granted Patent US 11,771,695
Granted Patent B2
US 11,771,695 · App. 17/478,274 · Granted Oct 3, 2023

Cannabinoid receptor modulators

Inventors: Jayant Thatte (San Diego, CA); Anthony C. Blackburn (San Diego, CA); Sangdon Han (San Diego, CA); Robert M. Jones (San Diego, CA); Jae-Kyu Jung (San Diego, CA); Antonio Garrido Montalban (San Diego, CA); Biman B. Pal (San Diego, CA); Jaimie Karyn Rueter (San Diego, CA); Sonja Strah-Pleynet (Newton, MA); Lars Thoresen (San Diego, CA); Yifeng Xiong (San Diego, CA); Dawei Yue (San Diego, CA); Xiuwen Zhu (San Diego, CA)
Assignee: Arena Pharmaceuticals, Inc.
A61K31/497A61K31/13A61K31/416A61K31/4439A61K31/485A61K31/675A61K45/06C07D231/54C07D401/04C07D401/14C07D403/04C07D405/14C07F9/65583
View Patent ↗
Loading inventors, assignments & file history…
Monitor This Case
Get email alerts when status or documents change.
Order Certified Copies
Most orders are placed with the USPTO same day — all within 24 business hours.
Order via The Patent Place →
Pre-filled with this patent's details
Quick Facts
Patent No.
US 11,771,695
App. No.
17/478,274
Granted
Oct 3, 2023
Kind
B2
Abstract

Provided are certain methods useful in the treatment of pain comprising administering a compound of Formula Ia and pharmaceutical compositions thereof that modulate the activity of the cannabinoid CB 2 receptor;

Claims (14)

1. A method for the management of pain in an individual in need thereof, comprising administering to said individual, a composition comprising a compound which is:

and one or more known pharmaceutical agents selected from: analgesic agents, antidiabetic agents, osteoarthritis agents, and anticancer agents; and a pharmaceutically acceptable carrier;

wherein the pain is chosen from: bone and joint pain, pain associated with osteoarthritis, hyperalgesia, allodynia, inflammatory pain, inflammatory hyperalgesia, neuropathic pain, neuropathic hyperalgesia, acute nociception, muscle pain, dental pain, migraine and other headache pain, pain that occurs as an adverse effect of therapeutics in an individual, and pain associated with a disorder selected from: cancer, multiple sclerosis, allergic reactions, nephritic syndrome, scleroderma, thyroiditis, diabetic neuropathy, fibromyalgia, HIV related-neuropathy, sciatica, and an autoimmune condition.

2. The method according to claim 1 , wherein the analgesic agent is chosen from non-opioid drugs, opioid drugs, and co-analgesic medications.

3. The method according to claim 2 , wherein the non-opioid drug is chosen from non steroidal anti-inflammatory agents, choline magnesium trisalicylate, sulfasalazine, olsalazin, phenacetin, tenoxicam, phenylbutazone, oxyphenthartazone, tapentadol, celecoxib, etoricoxib, lumiracoxib, rofecoxib, parecoxib, and ziconotide.

4. The method according to claim 3 , wherein the non steroidal anti-inflammatory agent is chosen from acemetacin, acetaminophen, aminoprofen, aspirin, benoxaprofen, bucloxic acid, carprofen, choline magnesium salicylate, choline salicylate, clidanac, diclofenac, diflunisal, diflurisal, etodolac, fenoprofen, fenoprofen calcium, fentiazac, flosulide, flubufen, flufenamic acid, flufenisal, flurbiprofen, fluprofen, ibuprofen, indoprofen, indomethacin, isoxicam, ketoprofen, ketorolac tromethamine, lornoxicam, magnesium salicylate, meclofenamic acid, meclofenamate sodium, mefenamic acid, meloxicam, muroprofen, nabumetone, naproxen, nepafenac, niflumic acid, nimesulide, oxaprozin, oxpinac, piroprofen, piroxicam, pramoprofen, ramifenazone, salsalate, salicylsalicylic acid, sodium salicylate, sudoxicam, sulindac, suprofen, tiaprofenic acid, tiopinac, tolfenamic acid, tolmetin, trioxaprofen, zidometacin, and zomepirac.

5. The method according to claim 2 , wherein the opioid drug is chosen from:

alfentanil, allylprodine, alphaprodine, anileridine, apomorphine, benzylmorphine, bezitramide, buprenorphine, butorphanol, clonitazene, codeine, desomorphine, dextromoramide, dextropropoxyphene, dezocine, diampromide, diamorphone, dihydrocodeine, dihydrocodeinone enol acetate, dihydromorphine, dilaudid, dimenoxadol, dimepheptanol, dimethylthiambutene, dioxaphetyl butyrate, dipipanone, eptazocine, ethoheptazine, ethylmethylthiambutene, ethylmorphine, etonitazene, fentanyl, heroin, hydrocodeine, hydrocodone, hydromorphone, hydroxypethidine, isomethadone, ketobemidone, levallorphan, levorphanol, levophenacylmorphan, lofentanil, meperidine, meptazinol, metazocine, methadone, metopon, 6-monoacetylmorphine, morphine, morphine-6-glucuronide, myrophine, nalbuphine, narceine, nicomorphine, norlevorphanol, normethadone, nalorphine, normorphine, norpipanone, noscapine, opium, oxycodone, oxymorphone, papavereturn, papverine, pentazocine, pethidine, phenadoxone, phenomorphan, phenazocine, phenoperidine, piminodine, piritramide, proheptazine, promedol, properidine, propiram, propoxyphene, sufentanil, tilidine, and tramadol.

6. The method according to claim 1 , wherein the analgesic agent comprises an NSAID and an opioid drug.

7. The method according to claim 1 , wherein the analgesic agent is chosen from vicodin, percocet, norco, lorcet, darvocet, and percodan.

8. The method according to claim 1 , wherein the analgesic agent is a co-analgesic medication chosen from antidepressants, anti-anxiety medications, migraine medications, and gabapentin.

9. The method according to claim 1 , wherein the anticancer agent is chosen from eribulin mesylate, cabazitaxel, sipuleucel-T, degarelix, raloxifene, topotecan hydrochloride, ixabepilone, lapatinib, erlotinib, gefitinib, abarelix, leuprolide acetate, fulvestrant, letrozole, triptorelin pamoate, herceptin, nolvadex, photofrin, xeloda, letrozole, anastrozole, flutamide, gemcitabine HCl, docetaxel, goserelin acetate, bevacizumab, celecoxib, cetuximab, denosumab, ibandronic acid, thyrotropin alfa, trabectedin, and pemetrexed.

10. The method according to claim 1 , wherein the osteoarthritis agent is chosen from valdecoxib, meloxicam, etodolac, naproxen sodium, diacerhein, tetracycline, antimalarial therapies, Gen-S, JNJ-39439335, JNJ-42160443, JNS013, N-[5-tert-butyl-2,3-dihydro-1H-inden-1(R)-yl]-N′-(1H-indazol-4-yl)urea, SAR114137, MEDI-578, LY545694, 6,14-ethenomorphinan-7-methanol, 17-(cyclopropylmethyl)-α-(1,1-dimethylethyl)-4,5-epoxy-18,19-dihydro-3-hydroxy-6-methoxy-α-methyl-(αS,5α,7α)-hydrochloride, GRC 15300, benzamide, 3-[3-bromo-4-[(2,4-difluorophenyl)methoxy]-6-methyl-2-oxo-1(2H)-pyridinyl]-N,4-dimethyl-, ADX71943, ELI-216, 1H-pyrrolo[1,2-a]imidazole-2,5(3H,6H)-dione, dihydro-, diractin, XEN 402, CRB 0022, apitoxin, and etoricoxib.

11. The method according to claim 1 , wherein the compound is an anhydrous crystalline form of:

Assignments (1)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Sep 23, 2021
From: THATTE, JAYANT; BLACKBURN, ANTHONY C.; HAN, SANGDON; JONES, ROBERT M.; JUNG, JAE-KYU; MONTALBAN, ANTONIO GARRIDO; PAL, BIMAN B.; RUETER, JAIMIE KARYN; STRAH-PLEYNET, SONJA; THORESEN, LARS; XIONG, YIFENG; YUE, DAWEI
To: ARENA PHARMACEUTICALS, INC.
Reel/Frame 057576/0274 →
Continuity (7)
Continuation 16442734 · Jun 17, 2019
Continuation 15831742 · Dec 5, 2017
Continuation 15279576 · Sep 29, 2016
Continuation 14956586 · Dec 2, 2015
Continuation 14001131
Provisional Application 61446729 · Feb 25, 2011
Related Publication 20220241274A1 · Aug 4, 2022
Cited By (1)
US 12,201,633