JP2019527711A5 - - Google Patents
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- Publication number
- JP2019527711A5 JP2019527711A5 JP2019506721A JP2019506721A JP2019527711A5 JP 2019527711 A5 JP2019527711 A5 JP 2019527711A5 JP 2019506721 A JP2019506721 A JP 2019506721A JP 2019506721 A JP2019506721 A JP 2019506721A JP 2019527711 A5 JP2019527711 A5 JP 2019527711A5
- Authority
- JP
- Japan
- Prior art keywords
- composition
- weight
- composition according
- glycol
- rapamycin
- 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.)
- Pending
Links
- 239000000203 mixture Substances 0.000 claims description 50
- DNIAPMSPPWPWGF-UHFFFAOYSA-N Propylene glycol Chemical compound CC(O)CO DNIAPMSPPWPWGF-UHFFFAOYSA-N 0.000 claims description 24
- LYCAIKOWRPUZTN-UHFFFAOYSA-N Ethylene glycol Chemical compound OCCO LYCAIKOWRPUZTN-UHFFFAOYSA-N 0.000 claims description 20
- WGCNASOHLSPBMP-UHFFFAOYSA-N hydroxyacetaldehyde Natural products OCC=O WGCNASOHLSPBMP-UHFFFAOYSA-N 0.000 claims description 10
- 239000007788 liquid Substances 0.000 claims description 10
- ZAHRKKWIAAJSAO-UHFFFAOYSA-N rapamycin Natural products COCC(O)C(=C/C(C)C(=O)CC(OC(=O)C1CCCCN1C(=O)C(=O)C2(O)OC(CC(OC)C(=CC=CC=CC(C)CC(C)C(=O)C)C)CCC2C)C(C)CC3CCC(O)C(C3)OC)C ZAHRKKWIAAJSAO-UHFFFAOYSA-N 0.000 claims description 10
- QFJCIRLUMZQUOT-HPLJOQBZSA-N sirolimus Chemical compound C1C[C@@H](O)[C@H](OC)C[C@@H]1C[C@@H](C)[C@H]1OC(=O)[C@@H]2CCCCN2C(=O)C(=O)[C@](O)(O2)[C@H](C)CC[C@H]2C[C@H](OC)/C(C)=C/C=C/C=C/[C@@H](C)C[C@@H](C)C(=O)[C@H](OC)[C@H](O)/C(C)=C/[C@@H](C)C(=O)C1 QFJCIRLUMZQUOT-HPLJOQBZSA-N 0.000 claims description 10
- 229960002930 sirolimus Drugs 0.000 claims description 10
- CSCPPACGZOOCGX-UHFFFAOYSA-N Acetone Chemical compound CC(C)=O CSCPPACGZOOCGX-UHFFFAOYSA-N 0.000 claims description 9
- PEDCQBHIVMGVHV-UHFFFAOYSA-N Glycerine Chemical compound OCC(O)CO PEDCQBHIVMGVHV-UHFFFAOYSA-N 0.000 claims description 9
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 claims description 5
- 239000002202 Polyethylene glycol Substances 0.000 claims description 5
- 229920001223 polyethylene glycol Polymers 0.000 claims description 5
- 206010040882 skin lesion Diseases 0.000 claims description 5
- 231100000444 skin lesion Toxicity 0.000 claims description 5
- VBICKXHEKHSIBG-UHFFFAOYSA-N 1-monostearoylglycerol Chemical compound CCCCCCCCCCCCCCCCCC(=O)OCC(O)CO VBICKXHEKHSIBG-UHFFFAOYSA-N 0.000 claims description 4
- 208000003120 Angiofibroma Diseases 0.000 claims description 4
- 239000004322 Butylated hydroxytoluene Substances 0.000 claims description 4
- NLZUEZXRPGMBCV-UHFFFAOYSA-N Butylhydroxytoluene Chemical compound CC1=CC(C(C)(C)C)=C(O)C(C(C)(C)C)=C1 NLZUEZXRPGMBCV-UHFFFAOYSA-N 0.000 claims description 4
- 239000002033 PVDF binder Substances 0.000 claims description 4
- 208000026911 Tuberous sclerosis complex Diseases 0.000 claims description 4
- 235000010354 butylated hydroxytoluene Nutrition 0.000 claims description 4
- 229940095259 butylated hydroxytoluene Drugs 0.000 claims description 4
- 230000001815 facial effect Effects 0.000 claims description 4
- 229920002981 polyvinylidene fluoride Polymers 0.000 claims description 4
- 208000009999 tuberous sclerosis Diseases 0.000 claims description 4
- 206010027145 Melanocytic naevus Diseases 0.000 claims description 3
- 208000007256 Nevus Diseases 0.000 claims description 3
- 208000009443 Vascular Malformations Diseases 0.000 claims description 3
- RFVNOJDQRGSOEL-UHFFFAOYSA-N 2-hydroxyethyl octadecanoate Chemical compound CCCCCCCCCCCCCCCCCC(=O)OCCO RFVNOJDQRGSOEL-UHFFFAOYSA-N 0.000 claims description 2
- 208000031857 Campbell de Morgan spots Diseases 0.000 claims description 2
- FBPFZTCFMRRESA-FSIIMWSLSA-N D-Glucitol Natural products OC[C@H](O)[C@H](O)[C@@H](O)[C@H](O)CO FBPFZTCFMRRESA-FSIIMWSLSA-N 0.000 claims description 2
- 208000032541 Epidermal naevus Diseases 0.000 claims description 2
- 206010025219 Lymphangioma Diseases 0.000 claims description 2
- 201000002571 Melkersson-Rosenthal syndrome Diseases 0.000 claims description 2
- 208000003019 Neurofibromatosis 1 Diseases 0.000 claims description 2
- 208000024834 Neurofibromatosis type 1 Diseases 0.000 claims description 2
- 241000588769 Proteus <enterobacteria> Species 0.000 claims description 2
- 206010037649 Pyogenic granuloma Diseases 0.000 claims description 2
- 208000034541 Rare lymphatic malformation Diseases 0.000 claims description 2
- 206010043189 Telangiectasia Diseases 0.000 claims description 2
- 229940073669 ceteareth 20 Drugs 0.000 claims description 2
- 229940081733 cetearyl alcohol Drugs 0.000 claims description 2
- 208000010575 cherry hemangioma Diseases 0.000 claims description 2
- 239000006071 cream Substances 0.000 claims description 2
- AMTWCFIAVKBGOD-UHFFFAOYSA-N dioxosilane;methoxy-dimethyl-trimethylsilyloxysilane Chemical compound O=[Si]=O.CO[Si](C)(C)O[Si](C)(C)C AMTWCFIAVKBGOD-UHFFFAOYSA-N 0.000 claims description 2
- BEFDCLMNVWHSGT-UHFFFAOYSA-N ethenylcyclopentane Chemical compound C=CC1CCCC1 BEFDCLMNVWHSGT-UHFFFAOYSA-N 0.000 claims description 2
- 208000014402 familial multiple discoid fibromas Diseases 0.000 claims description 2
- 229940075507 glyceryl monostearate Drugs 0.000 claims description 2
- 201000011066 hemangioma Diseases 0.000 claims description 2
- WSFSSNUMVMOOMR-NJFSPNSNSA-N methanone Chemical compound O=[14CH2] WSFSSNUMVMOOMR-NJFSPNSNSA-N 0.000 claims description 2
- 239000001788 mono and diglycerides of fatty acids Substances 0.000 claims description 2
- GLDOVTGHNKAZLK-UHFFFAOYSA-N octadecan-1-ol Chemical compound CCCCCCCCCCCCCCCCCCO GLDOVTGHNKAZLK-UHFFFAOYSA-N 0.000 claims description 2
- 206010030983 oral lichen planus Diseases 0.000 claims description 2
- 208000023112 overgrowth syndrome Diseases 0.000 claims description 2
- 235000019271 petrolatum Nutrition 0.000 claims description 2
- 229960004063 propylene glycol Drugs 0.000 claims description 2
- 239000008213 purified water Substances 0.000 claims description 2
- 229940083037 simethicone Drugs 0.000 claims description 2
- 235000010199 sorbic acid Nutrition 0.000 claims description 2
- 239000004334 sorbic acid Substances 0.000 claims description 2
- 229940075582 sorbic acid Drugs 0.000 claims description 2
- 239000000600 sorbitol Substances 0.000 claims description 2
- 208000011580 syndromic disease Diseases 0.000 claims description 2
- 208000009056 telangiectasis Diseases 0.000 claims description 2
- 230000008719 thickening Effects 0.000 claims description 2
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Chemical compound O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 claims description 2
- 239000003871 white petrolatum Substances 0.000 claims description 2
- KFZMGEQAYNKOFK-UHFFFAOYSA-N Isopropanol Chemical compound CC(C)O KFZMGEQAYNKOFK-UHFFFAOYSA-N 0.000 claims 3
- 238000003745 diagnosis Methods 0.000 claims 2
- 235000019441 ethanol Nutrition 0.000 claims 2
- QELSKZZBTMNZEB-UHFFFAOYSA-N propylparaben Chemical compound CCCOC(=O)C1=CC=C(O)C=C1 QELSKZZBTMNZEB-UHFFFAOYSA-N 0.000 claims 2
- 229940022682 acetone Drugs 0.000 claims 1
- 239000000654 additive Substances 0.000 claims 1
- 238000006136 alcoholysis reaction Methods 0.000 claims 1
- AKGGYBADQZYZPD-UHFFFAOYSA-N benzyl acetone Natural products CC(=O)CCC1=CC=CC=C1 AKGGYBADQZYZPD-UHFFFAOYSA-N 0.000 claims 1
- 239000002304 perfume Substances 0.000 claims 1
- WVDDGKGOMKODPV-ZQBYOMGUSA-N phenyl(114C)methanol Chemical compound O[14CH2]C1=CC=CC=C1 WVDDGKGOMKODPV-ZQBYOMGUSA-N 0.000 claims 1
- 235000010232 propyl p-hydroxybenzoate Nutrition 0.000 claims 1
- 239000004405 propyl p-hydroxybenzoate Substances 0.000 claims 1
- 229960003415 propylparaben Drugs 0.000 claims 1
- 229940068196 placebo Drugs 0.000 description 2
- 239000000902 placebo Substances 0.000 description 2
- 230000000699 topical effect Effects 0.000 description 2
- 206010067193 Naevus flammeus Diseases 0.000 description 1
- 210000004204 blood vessel Anatomy 0.000 description 1
- 231100000673 dose–response relationship Toxicity 0.000 description 1
- 229940079593 drug Drugs 0.000 description 1
- 239000003814 drug Substances 0.000 description 1
- 239000000975 dye Substances 0.000 description 1
- 208000002026 familial multiple nevi flammei Diseases 0.000 description 1
- 239000003205 fragrance Substances 0.000 description 1
- 230000003902 lesion Effects 0.000 description 1
- 230000036244 malformation Effects 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201662372940P | 2016-08-10 | 2016-08-10 | |
| US62/372,940 | 2016-08-10 | ||
| PCT/US2017/046320 WO2018031789A1 (en) | 2016-08-10 | 2017-08-10 | Topical rapamycin therapy |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2019527711A JP2019527711A (ja) | 2019-10-03 |
| JP2019527711A5 true JP2019527711A5 (enExample) | 2020-08-20 |
Family
ID=59684091
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2019506721A Pending JP2019527711A (ja) | 2016-08-10 | 2017-08-10 | 局所ラパマイシン療法 |
Country Status (11)
| Country | Link |
|---|---|
| US (1) | US20190167649A1 (enExample) |
| EP (1) | EP3496712A1 (enExample) |
| JP (1) | JP2019527711A (enExample) |
| KR (1) | KR20190039220A (enExample) |
| CN (1) | CN109689053A (enExample) |
| AU (1) | AU2017311491A1 (enExample) |
| BR (1) | BR112019002689A2 (enExample) |
| CA (1) | CA3032473A1 (enExample) |
| MX (1) | MX2019001670A (enExample) |
| RU (1) | RU2019106483A (enExample) |
| WO (1) | WO2018031789A1 (enExample) |
Families Citing this family (10)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2018129364A1 (en) | 2017-01-06 | 2018-07-12 | Palvella Therapeutics Llc | Anhydrous compositions of mtor inhibitors and methods of use |
| US12109199B2 (en) | 2018-02-06 | 2024-10-08 | Georgetown University | Topical mTOR inhibitors for cutaneous proliferative and vascular conditions |
| EP3817743A4 (en) | 2018-07-02 | 2022-07-06 | Palvella Therapeutics, Inc. | ANHYDROUS COMPOSITIONS OF MTOR INHIBITORS AND METHODS OF USE |
| WO2020047342A1 (en) * | 2018-08-30 | 2020-03-05 | Chemistryrx | Sirolimus containing compositions |
| CN109431997B (zh) * | 2018-12-20 | 2021-06-04 | 武汉科福新药有限责任公司 | 一种雷帕霉素局部注射制剂及其制备方法 |
| AU2020226527A1 (en) | 2019-02-20 | 2021-10-14 | AI Therapeutics, Inc. | Topical rapamycin formulations and their use in treating facial angiofibromas and other skin disorders |
| WO2020175131A1 (ja) * | 2019-02-27 | 2020-09-03 | 国立大学法人大阪大学 | 脈管異常治療用外用剤 |
| US20230056335A1 (en) | 2020-01-24 | 2023-02-23 | Nobelpharma Co., Ltd. | Topical formulation containing rapamycin |
| AU2020277132B1 (en) * | 2020-11-24 | 2021-11-04 | Aft Pharmaceuticals Limited | A Rapamycin Composition |
| AU2023203871B1 (en) * | 2023-06-20 | 2024-07-25 | Aft Pharmaceuticals Ltd | A Rapamycin Method of Treatment and Composition |
Family Cites Families (12)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| GB9606452D0 (en) | 1996-03-27 | 1996-06-05 | Sandoz Ltd | Organic compounds |
| WO1998002441A2 (en) | 1996-07-12 | 1998-01-22 | Ariad Pharmaceuticals, Inc. | Non immunosuppressive antifungal rapalogs |
| GB9723669D0 (en) | 1997-11-07 | 1998-01-07 | Univ Aberdeen | Skin penetration enhancing components |
| EP1546369A4 (en) | 2002-08-12 | 2007-01-17 | Univ Michigan | DIAGNOSIS AND TREATMENT OF DISEASES THROUGH DEFECTS IN THE TUBEROUS SKLEROSEPFAD |
| AU2006218918A1 (en) | 2005-03-02 | 2006-09-08 | Wyeth | Purification of rapamycin |
| KR20140016439A (ko) | 2006-02-02 | 2014-02-07 | 노파르티스 아게 | 결절성 경화증의 치료 |
| US20120022095A1 (en) | 2010-06-24 | 2012-01-26 | Teng Joyce M C | Topical rapamycin for treatment of facial angiofibromas in tuberous sclerosis |
| WO2012142145A1 (en) * | 2011-04-12 | 2012-10-18 | Dow Pharmaceutical Sciences | Methods of treating skin conditions exhibiting telangiectasia |
| US10172789B2 (en) * | 2013-01-24 | 2019-01-08 | Palvella Therapeutics Llc | Compositions for transdermal delivery of mTOR inhibitors |
| HUP1400075A2 (hu) * | 2014-02-14 | 2015-08-28 | Druggability Technologies Ip Holdco Jersey Ltd | Sirolimus és származékainak komplexei, elõállítása és gyógyszerészeti kompozíciói |
| WO2017053222A1 (en) * | 2015-09-24 | 2017-03-30 | Drexel University | Novel compositions and methods for treating or preventing dermal disorders |
| CN105663027B (zh) * | 2016-04-01 | 2018-12-18 | 中国人民解放军广州军区武汉总医院 | 西罗莫司外用制剂、其制备方法及用途 |
-
2017
- 2017-08-10 US US16/324,274 patent/US20190167649A1/en not_active Abandoned
- 2017-08-10 WO PCT/US2017/046320 patent/WO2018031789A1/en not_active Ceased
- 2017-08-10 EP EP17755383.1A patent/EP3496712A1/en not_active Withdrawn
- 2017-08-10 CA CA3032473A patent/CA3032473A1/en not_active Abandoned
- 2017-08-10 BR BR112019002689A patent/BR112019002689A2/pt not_active IP Right Cessation
- 2017-08-10 MX MX2019001670A patent/MX2019001670A/es unknown
- 2017-08-10 RU RU2019106483A patent/RU2019106483A/ru unknown
- 2017-08-10 KR KR1020197006896A patent/KR20190039220A/ko not_active Ceased
- 2017-08-10 CN CN201780049324.6A patent/CN109689053A/zh active Pending
- 2017-08-10 JP JP2019506721A patent/JP2019527711A/ja active Pending
- 2017-08-10 AU AU2017311491A patent/AU2017311491A1/en not_active Abandoned
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