JP2014527964A5 - - Google Patents
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- JP2014527964A5 JP2014527964A5 JP2014529957A JP2014529957A JP2014527964A5 JP 2014527964 A5 JP2014527964 A5 JP 2014527964A5 JP 2014529957 A JP2014529957 A JP 2014529957A JP 2014529957 A JP2014529957 A JP 2014529957A JP 2014527964 A5 JP2014527964 A5 JP 2014527964A5
- Authority
- JP
- Japan
- Prior art keywords
- composition
- weight
- composition according
- methyl salicylate
- camphor
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Granted
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- 239000000203 mixture Substances 0.000 claims description 100
- OSWPMRLSEDHDFF-UHFFFAOYSA-N methyl salicylate Chemical compound COC(=O)C1=CC=CC=C1O OSWPMRLSEDHDFF-UHFFFAOYSA-N 0.000 claims description 66
- YKPUWZUDDOIDPM-SOFGYWHQSA-N capsaicin Chemical compound COC1=CC(CNC(=O)CCCC\C=C\C(C)C)=CC=C1O YKPUWZUDDOIDPM-SOFGYWHQSA-N 0.000 claims description 52
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 claims description 37
- 229960001047 methyl salicylate Drugs 0.000 claims description 33
- 239000000556 agonist Substances 0.000 claims description 30
- DSSYKIVIOFKYAU-XCBNKYQSSA-N (R)-camphor Chemical group C1C[C@@]2(C)C(=O)C[C@@H]1C2(C)C DSSYKIVIOFKYAU-XCBNKYQSSA-N 0.000 claims description 26
- 241000723346 Cinnamomum camphora Species 0.000 claims description 26
- 229960000846 camphor Drugs 0.000 claims description 26
- 229930008380 camphor Natural products 0.000 claims description 26
- NOOLISFMXDJSKH-UTLUCORTSA-N (+)-Neomenthol Chemical group CC(C)[C@@H]1CC[C@@H](C)C[C@@H]1O NOOLISFMXDJSKH-UTLUCORTSA-N 0.000 claims description 25
- NOOLISFMXDJSKH-UHFFFAOYSA-N DL-menthol Natural products CC(C)C1CCC(C)CC1O NOOLISFMXDJSKH-UHFFFAOYSA-N 0.000 claims description 25
- 229940041616 menthol Drugs 0.000 claims description 25
- ISWSIDIOOBJBQZ-UHFFFAOYSA-N Phenol Chemical compound OC1=CC=CC=C1 ISWSIDIOOBJBQZ-UHFFFAOYSA-N 0.000 claims description 23
- 230000000202 analgesic effect Effects 0.000 claims description 20
- 229960002504 capsaicin Drugs 0.000 claims description 13
- 235000017663 capsaicin Nutrition 0.000 claims description 13
- 241000124008 Mammalia Species 0.000 claims description 9
- 229960003742 phenol Drugs 0.000 claims description 9
- 102000003568 TRPV3 Human genes 0.000 claims description 8
- 101150043371 Trpv3 gene Proteins 0.000 claims description 8
- 239000000730 antalgic agent Substances 0.000 claims description 8
- 239000000041 non-steroidal anti-inflammatory agent Substances 0.000 claims description 8
- 229940021182 non-steroidal anti-inflammatory drug Drugs 0.000 claims description 8
- 229940080309 TRPM8 agonist Drugs 0.000 claims description 7
- 230000000699 topical effect Effects 0.000 claims description 7
- PEDCQBHIVMGVHV-UHFFFAOYSA-N Glycerine Chemical compound OCC(O)CO PEDCQBHIVMGVHV-UHFFFAOYSA-N 0.000 claims description 6
- 229940035676 analgesics Drugs 0.000 claims description 6
- YGSDEFSMJLZEOE-UHFFFAOYSA-M salicylate Chemical compound OC1=CC=CC=C1C([O-])=O YGSDEFSMJLZEOE-UHFFFAOYSA-M 0.000 claims description 6
- 229960001860 salicylate Drugs 0.000 claims description 6
- 206010006784 Burning sensation Diseases 0.000 claims description 5
- 206010015150 Erythema Diseases 0.000 claims description 5
- 231100000321 erythema Toxicity 0.000 claims description 5
- 239000007788 liquid Substances 0.000 claims description 5
- 239000001293 FEMA 3089 Substances 0.000 claims description 4
- WEEGYLXZBRQIMU-UHFFFAOYSA-N 1,8-cineole Natural products C1CC2CCC1(C)OC2(C)C WEEGYLXZBRQIMU-UHFFFAOYSA-N 0.000 claims description 2
- RCEFMOGVOYEGJN-UHFFFAOYSA-N 3-(2-hydroxyphenyl)-6-(3-nitrophenyl)-1,4-dihydropyrimidin-2-one Chemical compound OC1=CC=CC=C1N1C(=O)NC(C=2C=C(C=CC=2)[N+]([O-])=O)=CC1 RCEFMOGVOYEGJN-UHFFFAOYSA-N 0.000 claims description 2
- BSYNRYMUTXBXSQ-UHFFFAOYSA-N Aspirin Chemical compound CC(=O)OC1=CC=CC=C1C(O)=O BSYNRYMUTXBXSQ-UHFFFAOYSA-N 0.000 claims description 2
- WEEGYLXZBRQIMU-WAAGHKOSSA-N Eucalyptol Chemical compound C1C[C@H]2CC[C@]1(C)OC2(C)C WEEGYLXZBRQIMU-WAAGHKOSSA-N 0.000 claims description 2
- HEFNNWSXXWATRW-UHFFFAOYSA-N Ibuprofen Chemical compound CC(C)CC1=CC=C(C(C)C(O)=O)C=C1 HEFNNWSXXWATRW-UHFFFAOYSA-N 0.000 claims description 2
- CMWTZPSULFXXJA-UHFFFAOYSA-N Naproxen Natural products C1=C(C(C)C(O)=O)C=CC2=CC(OC)=CC=C21 CMWTZPSULFXXJA-UHFFFAOYSA-N 0.000 claims description 2
- 229960001138 acetylsalicylic acid Drugs 0.000 claims description 2
- 229940121363 anti-inflammatory agent Drugs 0.000 claims description 2
- 239000002260 anti-inflammatory agent Substances 0.000 claims description 2
- 239000003638 chemical reducing agent Substances 0.000 claims description 2
- 229960005233 cineole Drugs 0.000 claims description 2
- 229960001259 diclofenac Drugs 0.000 claims description 2
- DCOPUUMXTXDBNB-UHFFFAOYSA-N diclofenac Chemical compound OC(=O)CC1=CC=CC=C1NC1=C(Cl)C=CC=C1Cl DCOPUUMXTXDBNB-UHFFFAOYSA-N 0.000 claims description 2
- 229960001680 ibuprofen Drugs 0.000 claims description 2
- DKYWVDODHFEZIM-UHFFFAOYSA-N ketoprofen Chemical compound OC(=O)C(C)C1=CC=CC(C(=O)C=2C=CC=CC=2)=C1 DKYWVDODHFEZIM-UHFFFAOYSA-N 0.000 claims description 2
- 229960000991 ketoprofen Drugs 0.000 claims description 2
- 229960002009 naproxen Drugs 0.000 claims description 2
- CMWTZPSULFXXJA-VIFPVBQESA-N naproxen Chemical compound C1=C([C@H](C)C(O)=O)C=CC2=CC(OC)=CC=C21 CMWTZPSULFXXJA-VIFPVBQESA-N 0.000 claims description 2
- 239000004094 surface-active agent Substances 0.000 claims description 2
- 239000007864 aqueous solution Substances 0.000 claims 3
- 208000035824 paresthesia Diseases 0.000 claims 2
- 150000003902 salicylic acid esters Chemical class 0.000 claims 2
- 238000011200 topical administration Methods 0.000 claims 2
- 102000003610 TRPM8 Human genes 0.000 claims 1
- 101150111302 Trpm8 gene Proteins 0.000 claims 1
- 102000003566 TRPV1 Human genes 0.000 description 19
- 101150016206 Trpv1 gene Proteins 0.000 description 19
- 238000000034 method Methods 0.000 description 15
- 235000019441 ethanol Nutrition 0.000 description 9
- 208000002193 Pain Diseases 0.000 description 6
- 210000004126 nerve fiber Anatomy 0.000 description 4
- 230000003040 nociceptive effect Effects 0.000 description 4
- ZYUVGYBAPZYKSA-UHFFFAOYSA-N 5-(3-hydroxybutan-2-yl)-4-methylbenzene-1,3-diol Chemical compound CC(O)C(C)C1=CC(O)=CC(O)=C1C ZYUVGYBAPZYKSA-UHFFFAOYSA-N 0.000 description 3
- NNJVILVZKWQKPM-UHFFFAOYSA-N Lidocaine Chemical compound CCN(CC)CC(=O)NC1=C(C)C=CC=C1C NNJVILVZKWQKPM-UHFFFAOYSA-N 0.000 description 3
- -1 amethokine Chemical compound 0.000 description 3
- NHADDZMCASKINP-HTRCEHHLSA-N decarboxydihydrocitrinin Natural products C1=C(O)C(C)=C2[C@H](C)[C@@H](C)OCC2=C1O NHADDZMCASKINP-HTRCEHHLSA-N 0.000 description 3
- 229960004194 lidocaine Drugs 0.000 description 3
- 239000003589 local anesthetic agent Substances 0.000 description 3
- 230000008058 pain sensation Effects 0.000 description 3
- 230000003381 solubilizing effect Effects 0.000 description 3
- 208000003251 Pruritus Diseases 0.000 description 2
- ZPUCINDJVBIVPJ-LJISPDSOSA-N cocaine Chemical compound O([C@H]1C[C@@H]2CC[C@@H](N2C)[C@H]1C(=O)OC)C(=O)C1=CC=CC=C1 ZPUCINDJVBIVPJ-LJISPDSOSA-N 0.000 description 2
- 150000001875 compounds Chemical class 0.000 description 2
- 229960005015 local anesthetics Drugs 0.000 description 2
- 238000002156 mixing Methods 0.000 description 2
- 238000005303 weighing Methods 0.000 description 2
- ZKMNUMMKYBVTFN-HNNXBMFYSA-N (S)-ropivacaine Chemical compound CCCN1CCCC[C@H]1C(=O)NC1=C(C)C=CC=C1C ZKMNUMMKYBVTFN-HNNXBMFYSA-N 0.000 description 1
- LEBVLXFERQHONN-UHFFFAOYSA-N 1-butyl-N-(2,6-dimethylphenyl)piperidine-2-carboxamide Chemical compound CCCCN1CCCCC1C(=O)NC1=C(C)C=CC=C1C LEBVLXFERQHONN-UHFFFAOYSA-N 0.000 description 1
- 201000004624 Dermatitis Diseases 0.000 description 1
- 206010019233 Headaches Diseases 0.000 description 1
- 208000004454 Hyperalgesia Diseases 0.000 description 1
- 208000035154 Hyperesthesia Diseases 0.000 description 1
- XQFRJNBWHJMXHO-RRKCRQDMSA-N IDUR Chemical compound C1[C@H](O)[C@@H](CO)O[C@H]1N1C(=O)NC(=O)C(I)=C1 XQFRJNBWHJMXHO-RRKCRQDMSA-N 0.000 description 1
- 208000005615 Interstitial Cystitis Diseases 0.000 description 1
- 201000004681 Psoriasis Diseases 0.000 description 1
- 206010040030 Sensory loss Diseases 0.000 description 1
- 208000009205 Tinnitus Diseases 0.000 description 1
- 230000003444 anaesthetic effect Effects 0.000 description 1
- 230000002917 arthritic effect Effects 0.000 description 1
- 206010003246 arthritis Diseases 0.000 description 1
- 229960003150 bupivacaine Drugs 0.000 description 1
- 229960001747 cinchocaine Drugs 0.000 description 1
- PUFQVTATUTYEAL-UHFFFAOYSA-N cinchocaine Chemical compound C1=CC=CC2=NC(OCCCC)=CC(C(=O)NCCN(CC)CC)=C21 PUFQVTATUTYEAL-UHFFFAOYSA-N 0.000 description 1
- 238000004140 cleaning Methods 0.000 description 1
- 229960003920 cocaine Drugs 0.000 description 1
- 210000004207 dermis Anatomy 0.000 description 1
- 229960001193 diclofenac sodium Drugs 0.000 description 1
- 230000000694 effects Effects 0.000 description 1
- 210000000981 epithelium Anatomy 0.000 description 1
- 229930003935 flavonoid Natural products 0.000 description 1
- 150000002215 flavonoids Chemical class 0.000 description 1
- 235000017173 flavonoids Nutrition 0.000 description 1
- 238000009472 formulation Methods 0.000 description 1
- 231100000869 headache Toxicity 0.000 description 1
- 230000002757 inflammatory effect Effects 0.000 description 1
- 230000007803 itching Effects 0.000 description 1
- 229960004288 levobupivacaine Drugs 0.000 description 1
- LEBVLXFERQHONN-INIZCTEOSA-N levobupivacaine Chemical compound CCCCN1CCCC[C@H]1C(=O)NC1=C(C)C=CC=C1C LEBVLXFERQHONN-INIZCTEOSA-N 0.000 description 1
- 238000004519 manufacturing process Methods 0.000 description 1
- 229960002409 mepivacaine Drugs 0.000 description 1
- INWLQCZOYSRPNW-UHFFFAOYSA-N mepivacaine Chemical compound CN1CCCCC1C(=O)NC1=C(C)C=CC=C1C INWLQCZOYSRPNW-UHFFFAOYSA-N 0.000 description 1
- 208000004296 neuralgia Diseases 0.000 description 1
- 208000021722 neuropathic pain Diseases 0.000 description 1
- 229940005483 opioid analgesics Drugs 0.000 description 1
- 201000008482 osteoarthritis Diseases 0.000 description 1
- 229960001807 prilocaine Drugs 0.000 description 1
- MVFGUOIZUNYYSO-UHFFFAOYSA-N prilocaine Chemical compound CCCNC(C)C(=O)NC1=CC=CC=C1C MVFGUOIZUNYYSO-UHFFFAOYSA-N 0.000 description 1
- 229960004919 procaine Drugs 0.000 description 1
- MFDFERRIHVXMIY-UHFFFAOYSA-N procaine Chemical compound CCN(CC)CCOC(=O)C1=CC=C(N)C=C1 MFDFERRIHVXMIY-UHFFFAOYSA-N 0.000 description 1
- 206010039073 rheumatoid arthritis Diseases 0.000 description 1
- 206010039083 rhinitis Diseases 0.000 description 1
- 229960001549 ropivacaine Drugs 0.000 description 1
- JGMJQSFLQWGYMQ-UHFFFAOYSA-M sodium;2,6-dichloro-n-phenylaniline;acetate Chemical compound [Na+].CC([O-])=O.ClC1=CC=CC(Cl)=C1NC1=CC=CC=C1 JGMJQSFLQWGYMQ-UHFFFAOYSA-M 0.000 description 1
- 208000003265 stomatitis Diseases 0.000 description 1
- 208000011580 syndromic disease Diseases 0.000 description 1
- 231100000886 tinnitus Toxicity 0.000 description 1
- 239000012049 topical pharmaceutical composition Substances 0.000 description 1
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201161533120P | 2011-09-09 | 2011-09-09 | |
| US61/533,120 | 2011-09-09 | ||
| US201261642942P | 2012-05-04 | 2012-05-04 | |
| US61/642,942 | 2012-05-04 | ||
| PCT/US2012/054511 WO2013036961A1 (en) | 2011-09-09 | 2012-09-10 | A pain relief composition, comprising a trpv1 selective agonist, and manufacture and uses thereof |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2014527964A JP2014527964A (ja) | 2014-10-23 |
| JP2014527964A5 true JP2014527964A5 (https=) | 2015-11-05 |
| JP6228540B2 JP6228540B2 (ja) | 2017-11-08 |
Family
ID=46940596
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2014529957A Expired - Fee Related JP6228540B2 (ja) | 2011-09-09 | 2012-09-10 | Ｔｒｐｖ１選択的アゴニストを含む疼痛軽減組成物、ならびにその製造および使用 |
Country Status (9)
| Country | Link |
|---|---|
| US (5) | US8889659B2 (https=) |
| EP (2) | EP3388057B1 (https=) |
| JP (1) | JP6228540B2 (https=) |
| KR (1) | KR101769010B1 (https=) |
| CN (1) | CN104010635A (https=) |
| BR (1) | BR112014005358A8 (https=) |
| CA (1) | CA2854206C (https=) |
| MX (1) | MX347902B (https=) |
| WO (1) | WO2013036961A1 (https=) |
Families Citing this family (31)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP3388057B1 (en) * | 2011-09-09 | 2022-03-09 | Propella Therapeutics, Inc. | A pain relief composition, comprising a trpv1 selective agonist, and manufacture and uses thereof |
| AU2013341380B2 (en) | 2012-11-12 | 2018-04-26 | Propella Therapeutics, Inc. | Aqueous based capsaicinoid formulations, and treatment in combination with a corticosteroid |
| CN105848666A (zh) * | 2013-10-28 | 2016-08-10 | Atp研究有限公司 | 疼痛缓解制剂以及治疗方法 |
| US20160334391A1 (en) * | 2014-01-23 | 2016-11-17 | Biogaia Ab | Selection of Agents Modulating Gastrointestinal Pain |
| JP6580305B2 (ja) * | 2014-03-30 | 2019-09-25 | 小林製薬株式会社 | 外用医薬組成物 |
| JP6599083B2 (ja) * | 2014-03-30 | 2019-10-30 | 小林製薬株式会社 | 外用医薬組成物 |
| MX377377B (es) | 2014-04-15 | 2025-03-10 | Propella Therapeutics Inc | Composiciones tópicas para el alivio del dolor, manufactura y uso. |
| KR102413721B1 (ko) * | 2014-11-26 | 2022-06-27 | 건양대학교산학협력단 | 통증완화 성분이 포함된 알코올성 조성물, 및 이를 포함하는 알코올 스왑 |
| JP6508671B2 (ja) * | 2015-01-30 | 2019-05-08 | ハウスウェルネスフーズ株式会社 | トウガラシ抽出物及び／又はショウガ抽出物を含む組成物、ならびにその製造方法 |
| WO2017020125A1 (en) | 2015-07-31 | 2017-02-09 | Delivra Inc. | Transdermal formulations for delivery of capsaicinoids |
| FR3039991A1 (fr) * | 2015-08-12 | 2017-02-17 | Ab7 Innovation | Composition antidouleur comprenant un derive de l'acide salicylique |
| JP6948762B2 (ja) * | 2015-10-16 | 2021-10-13 | 株式会社マンダム | Ｔｒｐｖ１活性抑制剤作用増幅用組成物 |
| EP3405187A4 (en) * | 2016-01-22 | 2019-07-31 | Centrexion Therapeutics Corporation | SEQUENCING DOSAGE METHOD FOR CAPSAICN FOR THE TREATMENT OF MORTON NEUROM |
| KR102657458B1 (ko) | 2016-11-02 | 2024-04-12 | 센트렉시온 테라퓨틱스 코포레이션 | 안정한 수성의 캡사이신 주사 가능한 제형 및 이의 의학적 용도 |
| PT3534922T (pt) | 2016-11-04 | 2024-06-07 | Takeda Pharmaceuticals Co | Formulações de vírus adenoassociado |
| TWI776879B (zh) * | 2017-04-04 | 2022-09-11 | 日商花王股份有限公司 | 身體化妝料 |
| WO2018198029A1 (en) * | 2017-04-25 | 2018-11-01 | Azista Industries Pvt Ltd | Matrix adhesive patch and process for the preparation thereof |
| WO2019018769A1 (en) | 2017-07-20 | 2019-01-24 | Centrexion Therapeutics Corporation | METHODS AND COMPOSITIONS FOR THE TREATMENT OF PAIN USING CAPSAICINE |
| AU2019299964A1 (en) | 2018-07-11 | 2021-01-21 | Takeda Pharmaceutical Company Limited | AAV compositions |
| CA3138194A1 (en) | 2019-04-30 | 2020-11-05 | Bayer Healthcare Llc | Topical analgesic gel compositions |
| US12097186B2 (en) | 2019-04-30 | 2024-09-24 | Bayer Healthcare Llc | Topical analgesic compositions |
| CA3138193A1 (en) * | 2019-04-30 | 2020-11-05 | Bayer Healthcare Llc | Topical analgesic spray compositions |
| TWI845702B (zh) | 2019-06-11 | 2024-06-21 | 美商先進製藥公司 | 超氧化物歧化酶可溶纖維組成物 |
| ES2998817T3 (en) * | 2019-08-05 | 2025-02-21 | Cs Medica As | Topical formulations comprising cannabidiol, method of preparing the composition and use thereof |
| MX2022011400A (es) | 2020-03-17 | 2022-10-13 | Gruenenthal Gmbh | Aplicacion topica repetida de parche de capsaicina para usarse para tratar pacientes que no responden inicialmente al tratamiento. |
| KR20220164022A (ko) | 2020-04-03 | 2022-12-12 | 그뤼넨탈 게엠베하 | 캡사이신 패치의 반복된 국소 적용 요법 |
| CN113662739A (zh) * | 2021-08-20 | 2021-11-19 | 刘浩泉 | 一种冰敷贴及其制作方法 |
| CN118510495A (zh) * | 2022-01-07 | 2024-08-16 | 高露洁-棕榄公司 | 口腔凝胶组合物 |
| CN114652708B (zh) * | 2022-03-07 | 2024-04-26 | 宁波奇致年华医疗科技有限公司 | 一种治疗深部组织疼痛的组合物 |
| CN114917190A (zh) * | 2022-06-13 | 2022-08-19 | 郑州味千生物技术有限公司 | 用于掩盖苦味的产品 |
| WO2025129126A1 (en) * | 2023-12-14 | 2025-06-19 | Vm Therapeutics Llc | Topical formulations of calcium channel blockers |
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-
2012
- 2012-09-10 EP EP18161847.1A patent/EP3388057B1/en not_active Not-in-force
- 2012-09-10 EP EP12766516.4A patent/EP2753319B1/en not_active Not-in-force
- 2012-09-10 WO PCT/US2012/054511 patent/WO2013036961A1/en not_active Ceased
- 2012-09-10 MX MX2014002718A patent/MX347902B/es active IP Right Grant
- 2012-09-10 CN CN201280055002.XA patent/CN104010635A/zh active Pending
- 2012-09-10 KR KR1020147008331A patent/KR101769010B1/ko not_active Expired - Fee Related
- 2012-09-10 US US13/609,100 patent/US8889659B2/en not_active Expired - Fee Related
- 2012-09-10 BR BR112014005358A patent/BR112014005358A8/pt not_active Application Discontinuation
- 2012-09-10 JP JP2014529957A patent/JP6228540B2/ja not_active Expired - Fee Related
- 2012-09-10 CA CA2854206A patent/CA2854206C/en not_active Expired - Fee Related
-
2013
- 2013-03-12 US US13/797,494 patent/US8802736B2/en active Active
-
2014
- 2014-09-10 US US14/482,930 patent/US10821088B2/en active Active
-
2018
- 2018-05-07 US US15/972,625 patent/US20180250246A1/en not_active Abandoned
-
2020
- 2020-10-12 US US16/949,046 patent/US20210100759A1/en not_active Abandoned
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