CN111683649A - 基于烟酰胺衍生物的局部组合物 - Google Patents
基于烟酰胺衍生物的局部组合物 Download PDFInfo
- Publication number
- CN111683649A CN111683649A CN201880081650.XA CN201880081650A CN111683649A CN 111683649 A CN111683649 A CN 111683649A CN 201880081650 A CN201880081650 A CN 201880081650A CN 111683649 A CN111683649 A CN 111683649A
- Authority
- CN
- China
- Prior art keywords
- composition
- cycloalkyl
- acid
- skin
- human body
- 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 title claims abstract description 128
- 230000000699 topical effect Effects 0.000 title claims abstract description 15
- 150000005480 nicotinamides Chemical class 0.000 title description 2
- 150000001875 compounds Chemical class 0.000 claims abstract description 35
- 125000000753 cycloalkyl group Chemical group 0.000 claims abstract description 18
- 125000004432 carbon atom Chemical group C* 0.000 claims abstract description 11
- 230000008901 benefit Effects 0.000 claims description 21
- DFPAKSUCGFBDDF-UHFFFAOYSA-N Nicotinamide Chemical compound NC(=O)C1=CC=CN=C1 DFPAKSUCGFBDDF-UHFFFAOYSA-N 0.000 claims description 18
- 230000000845 anti-microbial effect Effects 0.000 claims description 18
- 229960003966 nicotinamide Drugs 0.000 claims description 12
- 235000005152 nicotinamide Nutrition 0.000 claims description 12
- 239000011570 nicotinamide Substances 0.000 claims description 12
- 102000044503 Antimicrobial Peptides Human genes 0.000 claims description 11
- 108700042778 Antimicrobial Peptides Proteins 0.000 claims description 11
- 239000004615 ingredient Substances 0.000 claims description 10
- 238000000034 method Methods 0.000 claims description 10
- 239000004599 antimicrobial Substances 0.000 claims description 8
- VFQXVTODMYMSMJ-UHFFFAOYSA-N isonicotinamide Chemical compound NC(=O)C1=CC=NC=C1 VFQXVTODMYMSMJ-UHFFFAOYSA-N 0.000 claims description 6
- IBBMAWULFFBRKK-UHFFFAOYSA-N picolinamide Chemical compound NC(=O)C1=CC=CC=N1 IBBMAWULFFBRKK-UHFFFAOYSA-N 0.000 claims description 6
- 230000001939 inductive effect Effects 0.000 claims description 4
- 230000000249 desinfective effect Effects 0.000 claims description 3
- 239000003910 polypeptide antibiotic agent Substances 0.000 claims description 3
- 230000028327 secretion Effects 0.000 claims description 3
- YMWUJEATGCHHMB-UHFFFAOYSA-N Dichloromethane Chemical compound ClCCl YMWUJEATGCHHMB-UHFFFAOYSA-N 0.000 description 27
- 210000003491 skin Anatomy 0.000 description 23
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 description 16
- 239000002585 base Substances 0.000 description 16
- 238000004519 manufacturing process Methods 0.000 description 15
- -1 alkali metal salt Chemical class 0.000 description 12
- 239000006071 cream Substances 0.000 description 12
- CADNNWJTVVPKGS-UHFFFAOYSA-N n-cyclopentylpyridine-3-carboxamide Chemical compound C=1C=CN=CC=1C(=O)NC1CCCC1 CADNNWJTVVPKGS-UHFFFAOYSA-N 0.000 description 12
- 239000000516 sunscreening agent Substances 0.000 description 12
- 230000008859 change Effects 0.000 description 11
- PAQZWJGSJMLPMG-UHFFFAOYSA-N 2,4,6-tripropyl-1,3,5,2$l^{5},4$l^{5},6$l^{5}-trioxatriphosphinane 2,4,6-trioxide Chemical compound CCCP1(=O)OP(=O)(CCC)OP(=O)(CCC)O1 PAQZWJGSJMLPMG-UHFFFAOYSA-N 0.000 description 10
- 210000004027 cell Anatomy 0.000 description 10
- OKKJLVBELUTLKV-UHFFFAOYSA-N Methanol Chemical compound OC OKKJLVBELUTLKV-UHFFFAOYSA-N 0.000 description 9
- 239000007788 liquid Substances 0.000 description 9
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 description 9
- XEKOWRVHYACXOJ-UHFFFAOYSA-N Ethyl acetate Chemical compound CCOC(C)=O XEKOWRVHYACXOJ-UHFFFAOYSA-N 0.000 description 8
- KFZMGEQAYNKOFK-UHFFFAOYSA-N Isopropanol Chemical compound CC(C)O KFZMGEQAYNKOFK-UHFFFAOYSA-N 0.000 description 8
- PVNIIMVLHYAWGP-UHFFFAOYSA-N Niacin Chemical compound OC(=O)C1=CC=CN=C1 PVNIIMVLHYAWGP-UHFFFAOYSA-N 0.000 description 8
- 239000002781 deodorant agent Substances 0.000 description 8
- 239000004205 dimethyl polysiloxane Substances 0.000 description 8
- 235000013870 dimethyl polysiloxane Nutrition 0.000 description 8
- 244000005700 microbiome Species 0.000 description 8
- 229920000435 poly(dimethylsiloxane) Polymers 0.000 description 8
- VYPSYNLAJGMNEJ-UHFFFAOYSA-N Silicium dioxide Chemical compound O=[Si]=O VYPSYNLAJGMNEJ-UHFFFAOYSA-N 0.000 description 7
- 229940008099 dimethicone Drugs 0.000 description 7
- 239000000194 fatty acid Substances 0.000 description 7
- 239000003755 preservative agent Substances 0.000 description 7
- 230000000475 sunscreen effect Effects 0.000 description 7
- 241000894006 Bacteria Species 0.000 description 6
- LYCAIKOWRPUZTN-UHFFFAOYSA-N Ethylene glycol Chemical compound OCCO LYCAIKOWRPUZTN-UHFFFAOYSA-N 0.000 description 6
- DNIAPMSPPWPWGF-UHFFFAOYSA-N Propylene glycol Chemical compound CC(O)CO DNIAPMSPPWPWGF-UHFFFAOYSA-N 0.000 description 6
- 235000014113 dietary fatty acids Nutrition 0.000 description 6
- MTHSVFCYNBDYFN-UHFFFAOYSA-N diethylene glycol Chemical compound OCCOCCO MTHSVFCYNBDYFN-UHFFFAOYSA-N 0.000 description 6
- 239000000284 extract Substances 0.000 description 6
- 229930195729 fatty acid Natural products 0.000 description 6
- 150000004665 fatty acids Chemical class 0.000 description 6
- IPCSVZSSVZVIGE-UHFFFAOYSA-N hexadecanoic acid Chemical compound CCCCCCCCCCCCCCCC(O)=O IPCSVZSSVZVIGE-UHFFFAOYSA-N 0.000 description 6
- 210000000214 mouth Anatomy 0.000 description 6
- 229920002379 silicone rubber Polymers 0.000 description 6
- 239000000243 solution Substances 0.000 description 6
- DFPAKSUCGFBDDF-ZQBYOMGUSA-N [14c]-nicotinamide Chemical compound N[14C](=O)C1=CC=CN=C1 DFPAKSUCGFBDDF-ZQBYOMGUSA-N 0.000 description 5
- 239000000969 carrier Substances 0.000 description 5
- 238000006243 chemical reaction Methods 0.000 description 5
- 239000003795 chemical substances by application Substances 0.000 description 5
- 229920006037 cross link polymer Polymers 0.000 description 5
- NZZIMKJIVMHWJC-UHFFFAOYSA-N dibenzoylmethane Chemical compound C=1C=CC=CC=1C(=O)CC(=O)C1=CC=CC=C1 NZZIMKJIVMHWJC-UHFFFAOYSA-N 0.000 description 5
- 210000002510 keratinocyte Anatomy 0.000 description 5
- 239000000463 material Substances 0.000 description 5
- 210000004761 scalp Anatomy 0.000 description 5
- 239000000344 soap Substances 0.000 description 5
- 239000002904 solvent Substances 0.000 description 5
- RTZKZFJDLAIYFH-UHFFFAOYSA-N Diethyl ether Chemical compound CCOCC RTZKZFJDLAIYFH-UHFFFAOYSA-N 0.000 description 4
- YBGZDTIWKVFICR-JLHYYAGUSA-N Octyl 4-methoxycinnamic acid Chemical compound CCCCC(CC)COC(=O)\C=C\C1=CC=C(OC)C=C1 YBGZDTIWKVFICR-JLHYYAGUSA-N 0.000 description 4
- GWEVSGVZZGPLCZ-UHFFFAOYSA-N Titan oxide Chemical compound O=[Ti]=O GWEVSGVZZGPLCZ-UHFFFAOYSA-N 0.000 description 4
- GSEJCLTVZPLZKY-UHFFFAOYSA-N Triethanolamine Chemical compound OCCN(CCO)CCO GSEJCLTVZPLZKY-UHFFFAOYSA-N 0.000 description 4
- 150000001298 alcohols Chemical class 0.000 description 4
- 238000002474 experimental method Methods 0.000 description 4
- 210000004209 hair Anatomy 0.000 description 4
- 229960003512 nicotinic acid Drugs 0.000 description 4
- 235000001968 nicotinic acid Nutrition 0.000 description 4
- 239000011664 nicotinic acid Substances 0.000 description 4
- FJKROLUGYXJWQN-UHFFFAOYSA-N papa-hydroxy-benzoic acid Natural products OC(=O)C1=CC=C(O)C=C1 FJKROLUGYXJWQN-UHFFFAOYSA-N 0.000 description 4
- 230000001717 pathogenic effect Effects 0.000 description 4
- 230000002335 preservative effect Effects 0.000 description 4
- YGSDEFSMJLZEOE-UHFFFAOYSA-N salicylic acid Chemical compound OC(=O)C1=CC=CC=C1O YGSDEFSMJLZEOE-UHFFFAOYSA-N 0.000 description 4
- 230000001225 therapeutic effect Effects 0.000 description 4
- 238000004809 thin layer chromatography Methods 0.000 description 4
- 229940088594 vitamin Drugs 0.000 description 4
- 229930003231 vitamin Natural products 0.000 description 4
- 235000013343 vitamin Nutrition 0.000 description 4
- 239000011782 vitamin Substances 0.000 description 4
- CSCPPACGZOOCGX-UHFFFAOYSA-N Acetone Chemical compound CC(C)=O CSCPPACGZOOCGX-UHFFFAOYSA-N 0.000 description 3
- 241000588724 Escherichia coli Species 0.000 description 3
- 241000233866 Fungi Species 0.000 description 3
- 235000021314 Palmitic acid Nutrition 0.000 description 3
- 235000021355 Stearic acid Nutrition 0.000 description 3
- 239000002537 cosmetic Substances 0.000 description 3
- NISGSNTVMOOSJQ-UHFFFAOYSA-N cyclopentanamine Chemical compound NC1CCCC1 NISGSNTVMOOSJQ-UHFFFAOYSA-N 0.000 description 3
- 229920001971 elastomer Polymers 0.000 description 3
- 239000000806 elastomer Substances 0.000 description 3
- 239000003974 emollient agent Substances 0.000 description 3
- 238000005516 engineering process Methods 0.000 description 3
- 235000019439 ethyl acetate Nutrition 0.000 description 3
- 239000000499 gel Substances 0.000 description 3
- BXWNKGSJHAJOGX-UHFFFAOYSA-N hexadecan-1-ol Chemical compound CCCCCCCCCCCCCCCCO BXWNKGSJHAJOGX-UHFFFAOYSA-N 0.000 description 3
- 230000002209 hydrophobic effect Effects 0.000 description 3
- 239000006210 lotion Substances 0.000 description 3
- WQEPLUUGTLDZJY-UHFFFAOYSA-N n-Pentadecanoic acid Natural products CCCCCCCCCCCCCCC(O)=O WQEPLUUGTLDZJY-UHFFFAOYSA-N 0.000 description 3
- QIQXTHQIDYTFRH-UHFFFAOYSA-N octadecanoic acid Chemical compound CCCCCCCCCCCCCCCCCC(O)=O QIQXTHQIDYTFRH-UHFFFAOYSA-N 0.000 description 3
- OQCDKBAXFALNLD-UHFFFAOYSA-N octadecanoic acid Natural products CCCCCCCC(C)CCCCCCCCC(O)=O OQCDKBAXFALNLD-UHFFFAOYSA-N 0.000 description 3
- 239000003921 oil Substances 0.000 description 3
- 235000019198 oils Nutrition 0.000 description 3
- 229920001296 polysiloxane Polymers 0.000 description 3
- 239000007787 solid Substances 0.000 description 3
- 239000008117 stearic acid Substances 0.000 description 3
- 239000002562 thickening agent Substances 0.000 description 3
- 239000007762 w/o emulsion Substances 0.000 description 3
- ULQISTXYYBZJSJ-UHFFFAOYSA-N 12-hydroxyoctadecanoic acid Chemical compound CCCCCCC(O)CCCCCCCCCCC(O)=O ULQISTXYYBZJSJ-UHFFFAOYSA-N 0.000 description 2
- XDOFQFKRPWOURC-UHFFFAOYSA-N 16-methylheptadecanoic acid Chemical compound CC(C)CCCCCCCCCCCCCCC(O)=O XDOFQFKRPWOURC-UHFFFAOYSA-N 0.000 description 2
- WXTMDXOMEHJXQO-UHFFFAOYSA-N 2,5-dihydroxybenzoic acid Chemical compound OC(=O)C1=CC(O)=CC=C1O WXTMDXOMEHJXQO-UHFFFAOYSA-N 0.000 description 2
- UWNADWZGEHDQAB-UHFFFAOYSA-N 2,5-dimethylhexane Chemical group CC(C)CCC(C)C UWNADWZGEHDQAB-UHFFFAOYSA-N 0.000 description 2
- OSCJHTSDLYVCQC-UHFFFAOYSA-N 2-ethylhexyl 4-[[4-[4-(tert-butylcarbamoyl)anilino]-6-[4-(2-ethylhexoxycarbonyl)anilino]-1,3,5-triazin-2-yl]amino]benzoate Chemical compound C1=CC(C(=O)OCC(CC)CCCC)=CC=C1NC1=NC(NC=2C=CC(=CC=2)C(=O)NC(C)(C)C)=NC(NC=2C=CC(=CC=2)C(=O)OCC(CC)CCCC)=N1 OSCJHTSDLYVCQC-UHFFFAOYSA-N 0.000 description 2
- QCDWFXQBSFUVSP-UHFFFAOYSA-N 2-phenoxyethanol Chemical compound OCCOC1=CC=CC=C1 QCDWFXQBSFUVSP-UHFFFAOYSA-N 0.000 description 2
- OSDLLIBGSJNGJE-UHFFFAOYSA-N 4-chloro-3,5-dimethylphenol Chemical compound CC1=CC(O)=CC(C)=C1Cl OSDLLIBGSJNGJE-UHFFFAOYSA-N 0.000 description 2
- 239000005995 Aluminium silicate Substances 0.000 description 2
- CIWBSHSKHKDKBQ-JLAZNSOCSA-N Ascorbic acid Chemical compound OC[C@H](O)[C@H]1OC(=O)C(O)=C1O CIWBSHSKHKDKBQ-JLAZNSOCSA-N 0.000 description 2
- UXVMQQNJUSDDNG-UHFFFAOYSA-L Calcium chloride Chemical compound [Cl-].[Cl-].[Ca+2] UXVMQQNJUSDDNG-UHFFFAOYSA-L 0.000 description 2
- RGHNJXZEOKUKBD-SQOUGZDYSA-N D-gluconic acid Chemical compound OC[C@@H](O)[C@@H](O)[C@H](O)[C@@H](O)C(O)=O RGHNJXZEOKUKBD-SQOUGZDYSA-N 0.000 description 2
- 208000001840 Dandruff Diseases 0.000 description 2
- 238000002965 ELISA Methods 0.000 description 2
- 241000194033 Enterococcus Species 0.000 description 2
- AEMRFAOFKBGASW-UHFFFAOYSA-N Glycolic acid Chemical compound OCC(O)=O AEMRFAOFKBGASW-UHFFFAOYSA-N 0.000 description 2
- QIGBRXMKCJKVMJ-UHFFFAOYSA-N Hydroquinone Chemical compound OC1=CC=C(O)C=C1 QIGBRXMKCJKVMJ-UHFFFAOYSA-N 0.000 description 2
- UQSXHKLRYXJYBZ-UHFFFAOYSA-N Iron oxide Chemical compound [Fe]=O UQSXHKLRYXJYBZ-UHFFFAOYSA-N 0.000 description 2
- 241000607142 Salmonella Species 0.000 description 2
- 241000191940 Staphylococcus Species 0.000 description 2
- 241000194017 Streptococcus Species 0.000 description 2
- PPBRXRYQALVLMV-UHFFFAOYSA-N Styrene Chemical compound C=CC1=CC=CC=C1 PPBRXRYQALVLMV-UHFFFAOYSA-N 0.000 description 2
- XLOMVQKBTHCTTD-UHFFFAOYSA-N Zinc monoxide Chemical compound [Zn]=O XLOMVQKBTHCTTD-UHFFFAOYSA-N 0.000 description 2
- 239000002253 acid Substances 0.000 description 2
- 239000000654 additive Substances 0.000 description 2
- 235000012211 aluminium silicate Nutrition 0.000 description 2
- 239000003963 antioxidant agent Substances 0.000 description 2
- 235000006708 antioxidants Nutrition 0.000 description 2
- 239000012298 atmosphere Substances 0.000 description 2
- XNEFYCZVKIDDMS-UHFFFAOYSA-N avobenzone Chemical compound C1=CC(OC)=CC=C1C(=O)CC(=O)C1=CC=C(C(C)(C)C)C=C1 XNEFYCZVKIDDMS-UHFFFAOYSA-N 0.000 description 2
- 229960000686 benzalkonium chloride Drugs 0.000 description 2
- 229960001950 benzethonium chloride Drugs 0.000 description 2
- UREZNYTWGJKWBI-UHFFFAOYSA-M benzethonium chloride Chemical compound [Cl-].C1=CC(C(C)(C)CC(C)(C)C)=CC=C1OCCOCC[N+](C)(C)CC1=CC=CC=C1 UREZNYTWGJKWBI-UHFFFAOYSA-M 0.000 description 2
- CADWTSSKOVRVJC-UHFFFAOYSA-N benzyl(dimethyl)azanium;chloride Chemical compound [Cl-].C[NH+](C)CC1=CC=CC=C1 CADWTSSKOVRVJC-UHFFFAOYSA-N 0.000 description 2
- 230000015572 biosynthetic process Effects 0.000 description 2
- 239000012267 brine Substances 0.000 description 2
- 238000004113 cell culture Methods 0.000 description 2
- 239000003086 colorant Substances 0.000 description 2
- CVSVTCORWBXHQV-UHFFFAOYSA-N creatine Chemical compound NC(=[NH2+])N(C)CC([O-])=O CVSVTCORWBXHQV-UHFFFAOYSA-N 0.000 description 2
- DDRJAANPRJIHGJ-UHFFFAOYSA-N creatinine Chemical compound CN1CC(=O)NC1=N DDRJAANPRJIHGJ-UHFFFAOYSA-N 0.000 description 2
- 239000012043 crude product Substances 0.000 description 2
- 239000012228 culture supernatant Substances 0.000 description 2
- PAFZNILMFXTMIY-UHFFFAOYSA-N cyclohexylamine Chemical compound NC1CCCCC1 PAFZNILMFXTMIY-UHFFFAOYSA-N 0.000 description 2
- SASYSVUEVMOWPL-NXVVXOECSA-N decyl oleate Chemical compound CCCCCCCCCCOC(=O)CCCCCCC\C=C/CCCCCCCC SASYSVUEVMOWPL-NXVVXOECSA-N 0.000 description 2
- 230000007123 defense Effects 0.000 description 2
- 208000002925 dental caries Diseases 0.000 description 2
- 239000007854 depigmenting agent Substances 0.000 description 2
- GUJOJGAPFQRJSV-UHFFFAOYSA-N dialuminum;dioxosilane;oxygen(2-);hydrate Chemical compound O.[O-2].[O-2].[O-2].[Al+3].[Al+3].O=[Si]=O.O=[Si]=O.O=[Si]=O.O=[Si]=O GUJOJGAPFQRJSV-UHFFFAOYSA-N 0.000 description 2
- NOPFSRXAKWQILS-UHFFFAOYSA-N docosan-1-ol Chemical compound CCCCCCCCCCCCCCCCCCCCCCO NOPFSRXAKWQILS-UHFFFAOYSA-N 0.000 description 2
- 230000001804 emulsifying effect Effects 0.000 description 2
- 239000000839 emulsion Substances 0.000 description 2
- 239000012530 fluid Substances 0.000 description 2
- 229910021485 fumed silica Inorganic materials 0.000 description 2
- 239000001963 growth medium Substances 0.000 description 2
- 239000003906 humectant Substances 0.000 description 2
- BJRNKVDFDLYUGJ-RMPHRYRLSA-N hydroquinone O-beta-D-glucopyranoside Chemical compound O[C@@H]1[C@@H](O)[C@H](O)[C@@H](CO)O[C@H]1OC1=CC=C(O)C=C1 BJRNKVDFDLYUGJ-RMPHRYRLSA-N 0.000 description 2
- 230000036039 immunity Effects 0.000 description 2
- 208000015181 infectious disease Diseases 0.000 description 2
- NLYAJNPCOHFWQQ-UHFFFAOYSA-N kaolin Chemical compound O.O.O=[Al]O[Si](=O)O[Si](=O)O[Al]=O NLYAJNPCOHFWQQ-UHFFFAOYSA-N 0.000 description 2
- JVTAAEKCZFNVCJ-UHFFFAOYSA-N lactic acid Chemical compound CC(O)C(O)=O JVTAAEKCZFNVCJ-UHFFFAOYSA-N 0.000 description 2
- 230000005923 long-lasting effect Effects 0.000 description 2
- 239000002609 medium Substances 0.000 description 2
- LXCFILQKKLGQFO-UHFFFAOYSA-N methylparaben Chemical compound COC(=O)C1=CC=C(O)C=C1 LXCFILQKKLGQFO-UHFFFAOYSA-N 0.000 description 2
- BDJRBEYXGGNYIS-UHFFFAOYSA-N nonanedioic acid Chemical compound OC(=O)CCCCCCCC(O)=O BDJRBEYXGGNYIS-UHFFFAOYSA-N 0.000 description 2
- GLDOVTGHNKAZLK-UHFFFAOYSA-N octadecan-1-ol Chemical compound CCCCCCCCCCCCCCCCCCO GLDOVTGHNKAZLK-UHFFFAOYSA-N 0.000 description 2
- 229960001679 octinoxate Drugs 0.000 description 2
- 239000003605 opacifier Substances 0.000 description 2
- 229960005323 phenoxyethanol Drugs 0.000 description 2
- 230000000704 physical effect Effects 0.000 description 2
- 229920000642 polymer Polymers 0.000 description 2
- 229920005862 polyol Polymers 0.000 description 2
- 150000003077 polyols Chemical class 0.000 description 2
- 239000000843 powder Substances 0.000 description 2
- 239000000047 product Substances 0.000 description 2
- QELSKZZBTMNZEB-UHFFFAOYSA-N propylparaben Chemical compound CCCOC(=O)C1=CC=C(O)C=C1 QELSKZZBTMNZEB-UHFFFAOYSA-N 0.000 description 2
- LXNHXLLTXMVWPM-UHFFFAOYSA-N pyridoxine Chemical compound CC1=NC=C(CO)C(CO)=C1O LXNHXLLTXMVWPM-UHFFFAOYSA-N 0.000 description 2
- 239000011541 reaction mixture Substances 0.000 description 2
- 230000008439 repair process Effects 0.000 description 2
- 229960004889 salicylic acid Drugs 0.000 description 2
- 239000000377 silicon dioxide Substances 0.000 description 2
- 229920002545 silicone oil Polymers 0.000 description 2
- 239000011734 sodium Substances 0.000 description 2
- 229910052938 sodium sulfate Inorganic materials 0.000 description 2
- HPALAKNZSZLMCH-UHFFFAOYSA-M sodium;chloride;hydrate Chemical compound O.[Na+].[Cl-] HPALAKNZSZLMCH-UHFFFAOYSA-M 0.000 description 2
- 239000000126 substance Substances 0.000 description 2
- 150000005846 sugar alcohols Polymers 0.000 description 2
- 238000003786 synthesis reaction Methods 0.000 description 2
- 239000004408 titanium dioxide Substances 0.000 description 2
- 125000000391 vinyl group Chemical group [H]C([*])=C([H])[H] 0.000 description 2
- 229920002554 vinyl polymer Polymers 0.000 description 2
- 229940043810 zinc pyrithione Drugs 0.000 description 2
- PICXIOQBANWBIZ-UHFFFAOYSA-N zinc;1-oxidopyridine-2-thione Chemical compound [Zn+2].[O-]N1C=CC=CC1=S.[O-]N1C=CC=CC1=S PICXIOQBANWBIZ-UHFFFAOYSA-N 0.000 description 2
- NOOLISFMXDJSKH-UTLUCORTSA-N (+)-Neomenthol Chemical compound CC(C)[C@@H]1CC[C@@H](C)C[C@@H]1O NOOLISFMXDJSKH-UTLUCORTSA-N 0.000 description 1
- ALSTYHKOOCGGFT-KTKRTIGZSA-N (9Z)-octadecen-1-ol Chemical compound CCCCCCCC\C=C/CCCCCCCCO ALSTYHKOOCGGFT-KTKRTIGZSA-N 0.000 description 1
- OYHQOLUKZRVURQ-NTGFUMLPSA-N (9Z,12Z)-9,10,12,13-tetratritiooctadeca-9,12-dienoic acid Chemical compound C(CCCCCCC\C(=C(/C\C(=C(/CCCCC)\[3H])\[3H])\[3H])\[3H])(=O)O OYHQOLUKZRVURQ-NTGFUMLPSA-N 0.000 description 1
- BIDDLDNGQCUOJQ-KAMYIIQDSA-N (z)-2,3-diphenylprop-2-enoic acid Chemical compound C=1C=CC=CC=1/C(C(=O)O)=C/C1=CC=CC=C1 BIDDLDNGQCUOJQ-KAMYIIQDSA-N 0.000 description 1
- QMMJWQMCMRUYTG-UHFFFAOYSA-N 1,2,4,5-tetrachloro-3-(trifluoromethyl)benzene Chemical compound FC(F)(F)C1=C(Cl)C(Cl)=CC(Cl)=C1Cl QMMJWQMCMRUYTG-UHFFFAOYSA-N 0.000 description 1
- 229940031723 1,2-octanediol Drugs 0.000 description 1
- 150000005207 1,3-dihydroxybenzenes Chemical class 0.000 description 1
- LALVCWMSKLEQMK-UHFFFAOYSA-N 1-phenyl-3-(4-propan-2-ylphenyl)propane-1,3-dione Chemical compound C1=CC(C(C)C)=CC=C1C(=O)CC(=O)C1=CC=CC=C1 LALVCWMSKLEQMK-UHFFFAOYSA-N 0.000 description 1
- 229940114072 12-hydroxystearic acid Drugs 0.000 description 1
- FPIPGXGPPPQFEQ-UHFFFAOYSA-N 13-cis retinol Natural products OCC=C(C)C=CC=C(C)C=CC1=C(C)CCCC1(C)C FPIPGXGPPPQFEQ-UHFFFAOYSA-N 0.000 description 1
- LGEZTMRIZWCDLW-UHFFFAOYSA-N 14-methylpentadecyl octadecanoate Chemical compound CCCCCCCCCCCCCCCCCC(=O)OCCCCCCCCCCCCCC(C)C LGEZTMRIZWCDLW-UHFFFAOYSA-N 0.000 description 1
- HDIFHQMREAYYJW-FMIVXFBMSA-N 2,3-dihydroxypropyl (e)-12-hydroxyoctadec-9-enoate Chemical compound CCCCCCC(O)C\C=C\CCCCCCCC(=O)OCC(O)CO HDIFHQMREAYYJW-FMIVXFBMSA-N 0.000 description 1
- FLPJVCMIKUWSDR-UHFFFAOYSA-N 2-(4-formylphenoxy)acetamide Chemical compound NC(=O)COC1=CC=C(C=O)C=C1 FLPJVCMIKUWSDR-UHFFFAOYSA-N 0.000 description 1
- ZNQVEEAIQZEUHB-UHFFFAOYSA-N 2-ethoxyethanol Chemical compound CCOCCO ZNQVEEAIQZEUHB-UHFFFAOYSA-N 0.000 description 1
- RFVNOJDQRGSOEL-UHFFFAOYSA-N 2-hydroxyethyl octadecanoate Chemical compound CCCCCCCCCCCCCCCCCC(=O)OCCO RFVNOJDQRGSOEL-UHFFFAOYSA-N 0.000 description 1
- JKRDADVRIYVCCY-UHFFFAOYSA-N 2-hydroxyoctanoic acid Chemical compound CCCCCCC(O)C(O)=O JKRDADVRIYVCCY-UHFFFAOYSA-N 0.000 description 1
- OJIBJRXMHVZPLV-UHFFFAOYSA-N 2-methylpropyl hexadecanoate Chemical compound CCCCCCCCCCCCCCCC(=O)OCC(C)C OJIBJRXMHVZPLV-UHFFFAOYSA-N 0.000 description 1
- GTJOHISYCKPIMT-UHFFFAOYSA-N 2-methylundecane Chemical compound CCCCCCCCCC(C)C GTJOHISYCKPIMT-UHFFFAOYSA-N 0.000 description 1
- CYDQOEWLBCCFJZ-UHFFFAOYSA-N 4-(4-fluorophenyl)oxane-4-carboxylic acid Chemical compound C=1C=C(F)C=CC=1C1(C(=O)O)CCOCC1 CYDQOEWLBCCFJZ-UHFFFAOYSA-N 0.000 description 1
- HIQIXEFWDLTDED-UHFFFAOYSA-N 4-hydroxy-1-piperidin-4-ylpyrrolidin-2-one Chemical compound O=C1CC(O)CN1C1CCNCC1 HIQIXEFWDLTDED-UHFFFAOYSA-N 0.000 description 1
- 229940090248 4-hydroxybenzoic acid Drugs 0.000 description 1
- 150000005422 4-hydroxybenzoic acid derivatives Chemical class 0.000 description 1
- 239000002677 5-alpha reductase inhibitor Substances 0.000 description 1
- AMEMLELAMQEAIA-UHFFFAOYSA-N 6-(tert-butyl)thieno[3,2-d]pyrimidin-4(3H)-one Chemical compound N1C=NC(=O)C2=C1C=C(C(C)(C)C)S2 AMEMLELAMQEAIA-UHFFFAOYSA-N 0.000 description 1
- KGKQNDQDVZQTAG-UHFFFAOYSA-N 8-methylnonyl 2,2-dimethylpropanoate Chemical compound CC(C)CCCCCCCOC(=O)C(C)(C)C KGKQNDQDVZQTAG-UHFFFAOYSA-N 0.000 description 1
- 244000144927 Aloe barbadensis Species 0.000 description 1
- 235000002961 Aloe barbadensis Nutrition 0.000 description 1
- QGZKDVFQNNGYKY-UHFFFAOYSA-O Ammonium Chemical compound [NH4+] QGZKDVFQNNGYKY-UHFFFAOYSA-O 0.000 description 1
- 239000004251 Ammonium lactate Substances 0.000 description 1
- 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 description 1
- 235000005979 Citrus limon Nutrition 0.000 description 1
- 244000131522 Citrus pyriformis Species 0.000 description 1
- ZZZCUOFIHGPKAK-UHFFFAOYSA-N D-erythro-ascorbic acid Natural products OCC1OC(=O)C(O)=C1O ZZZCUOFIHGPKAK-UHFFFAOYSA-N 0.000 description 1
- RGHNJXZEOKUKBD-UHFFFAOYSA-N D-gluconic acid Natural products OCC(O)C(O)C(O)C(O)C(O)=O RGHNJXZEOKUKBD-UHFFFAOYSA-N 0.000 description 1
- NOOLISFMXDJSKH-UHFFFAOYSA-N DL-menthol Natural products CC(C)C1CCC(C)CC1O NOOLISFMXDJSKH-UHFFFAOYSA-N 0.000 description 1
- PYGXAGIECVVIOZ-UHFFFAOYSA-N Dibutyl decanedioate Chemical compound CCCCOC(=O)CCCCCCCCC(=O)OCCCC PYGXAGIECVVIOZ-UHFFFAOYSA-N 0.000 description 1
- 238000008157 ELISA kit Methods 0.000 description 1
- 239000004266 EU approved firming agent Substances 0.000 description 1
- AFSDNFLWKVMVRB-UHFFFAOYSA-N Ellagic acid Chemical compound OC1=C(O)C(OC2=O)=C3C4=C2C=C(O)C(O)=C4OC(=O)C3=C1 AFSDNFLWKVMVRB-UHFFFAOYSA-N 0.000 description 1
- ATJXMQHAMYVHRX-CPCISQLKSA-N Ellagic acid Natural products OC1=C(O)[C@H]2OC(=O)c3cc(O)c(O)c4OC(=O)C(=C1)[C@H]2c34 ATJXMQHAMYVHRX-CPCISQLKSA-N 0.000 description 1
- 229920002079 Ellagic acid Polymers 0.000 description 1
- 108090000790 Enzymes Proteins 0.000 description 1
- 102000004190 Enzymes Human genes 0.000 description 1
- FPVVYTCTZKCSOJ-UHFFFAOYSA-N Ethylene glycol distearate Chemical compound CCCCCCCCCCCCCCCCCC(=O)OCCOC(=O)CCCCCCCCCCCCCCCCC FPVVYTCTZKCSOJ-UHFFFAOYSA-N 0.000 description 1
- 208000018522 Gastrointestinal disease Diseases 0.000 description 1
- 241000238631 Hexapoda Species 0.000 description 1
- CMBYOWLFQAFZCP-UHFFFAOYSA-N Hexyl dodecanoate Chemical compound CCCCCCCCCCCC(=O)OCCCCCC CMBYOWLFQAFZCP-UHFFFAOYSA-N 0.000 description 1
- 241000282412 Homo Species 0.000 description 1
- DGAQECJNVWCQMB-PUAWFVPOSA-M Ilexoside XXIX Chemical compound C[C@@H]1CC[C@@]2(CC[C@@]3(C(=CC[C@H]4[C@]3(CC[C@@H]5[C@@]4(CC[C@@H](C5(C)C)OS(=O)(=O)[O-])C)C)[C@@H]2[C@]1(C)O)C)C(=O)O[C@H]6[C@@H]([C@H]([C@@H]([C@H](O6)CO)O)O)O.[Na+] DGAQECJNVWCQMB-PUAWFVPOSA-M 0.000 description 1
- 238000012404 In vitro experiment Methods 0.000 description 1
- SGVYKUFIHHTIFL-UHFFFAOYSA-N Isobutylhexyl Natural products CCCCCCCC(C)C SGVYKUFIHHTIFL-UHFFFAOYSA-N 0.000 description 1
- 241000588748 Klebsiella Species 0.000 description 1
- DOUMFZQKYFQNTF-WUTVXBCWSA-N Labiatenic acid Natural products C([C@H](C(=O)O)OC(=O)\C=C\C=1C=C(O)C(O)=CC=1)C1=CC=C(O)C(O)=C1 DOUMFZQKYFQNTF-WUTVXBCWSA-N 0.000 description 1
- 239000004166 Lanolin Substances 0.000 description 1
- 241001465754 Metazoa Species 0.000 description 1
- 240000000249 Morus alba Species 0.000 description 1
- 235000008708 Morus alba Nutrition 0.000 description 1
- 240000009023 Myrrhis odorata Species 0.000 description 1
- 235000007265 Myrrhis odorata Nutrition 0.000 description 1
- 239000007832 Na2SO4 Substances 0.000 description 1
- 241000772415 Neovison vison Species 0.000 description 1
- 235000019483 Peanut oil Nutrition 0.000 description 1
- 239000004264 Petrolatum Substances 0.000 description 1
- 235000012550 Pimpinella anisum Nutrition 0.000 description 1
- 239000004698 Polyethylene Substances 0.000 description 1
- 239000002202 Polyethylene glycol Substances 0.000 description 1
- XBDQKXXYIPTUBI-UHFFFAOYSA-N Propionic acid Chemical class CCC(O)=O XBDQKXXYIPTUBI-UHFFFAOYSA-N 0.000 description 1
- 208000003251 Pruritus Diseases 0.000 description 1
- 235000019484 Rapeseed oil Nutrition 0.000 description 1
- ZZAFFYPNLYCDEP-HNNXBMFYSA-N Rosmarinsaeure Natural products OC(=O)[C@H](Cc1cccc(O)c1O)OC(=O)C=Cc2ccc(O)c(O)c2 ZZAFFYPNLYCDEP-HNNXBMFYSA-N 0.000 description 1
- 229940122511 Sebum inhibitor Drugs 0.000 description 1
- 244000000231 Sesamum indicum Species 0.000 description 1
- 235000003434 Sesamum indicum Nutrition 0.000 description 1
- 241000607768 Shigella Species 0.000 description 1
- 206010040799 Skin atrophy Diseases 0.000 description 1
- 206010040844 Skin exfoliation Diseases 0.000 description 1
- PMZURENOXWZQFD-UHFFFAOYSA-L Sodium Sulfate Chemical compound [Na+].[Na+].[O-]S([O-])(=O)=O PMZURENOXWZQFD-UHFFFAOYSA-L 0.000 description 1
- 239000004288 Sodium dehydroacetate Substances 0.000 description 1
- 229920002125 Sokalan® Polymers 0.000 description 1
- 241000191967 Staphylococcus aureus Species 0.000 description 1
- 229920002472 Starch Polymers 0.000 description 1
- XEFQLINVKFYRCS-UHFFFAOYSA-N Triclosan Chemical compound OC1=CC(Cl)=CC=C1OC1=CC=C(Cl)C=C1Cl XEFQLINVKFYRCS-UHFFFAOYSA-N 0.000 description 1
- 241000700605 Viruses Species 0.000 description 1
- FPIPGXGPPPQFEQ-BOOMUCAASA-N Vitamin A Natural products OC/C=C(/C)\C=C\C=C(\C)/C=C/C1=C(C)CCCC1(C)C FPIPGXGPPPQFEQ-BOOMUCAASA-N 0.000 description 1
- 229930003779 Vitamin B12 Natural products 0.000 description 1
- 229930003268 Vitamin C Natural products 0.000 description 1
- DPXJVFZANSGRMM-UHFFFAOYSA-N acetic acid;2,3,4,5,6-pentahydroxyhexanal;sodium Chemical compound [Na].CC(O)=O.OCC(O)C(O)C(O)C(O)C=O DPXJVFZANSGRMM-UHFFFAOYSA-N 0.000 description 1
- 229940048299 acetylated lanolin alcohols Drugs 0.000 description 1
- 229910052783 alkali metal Inorganic materials 0.000 description 1
- 125000005907 alkyl ester group Chemical group 0.000 description 1
- FPIPGXGPPPQFEQ-OVSJKPMPSA-N all-trans-retinol Chemical compound OC\C=C(/C)\C=C\C=C(/C)\C=C\C1=C(C)CCCC1(C)C FPIPGXGPPPQFEQ-OVSJKPMPSA-N 0.000 description 1
- 235000011399 aloe vera Nutrition 0.000 description 1
- 235000014104 aloe vera supplement Nutrition 0.000 description 1
- PNEYBMLMFCGWSK-UHFFFAOYSA-N aluminium oxide Inorganic materials [O-2].[O-2].[O-2].[Al+3].[Al+3] PNEYBMLMFCGWSK-UHFFFAOYSA-N 0.000 description 1
- 229910000323 aluminium silicate Inorganic materials 0.000 description 1
- 150000001408 amides Chemical group 0.000 description 1
- 229940059265 ammonium lactate Drugs 0.000 description 1
- 235000019286 ammonium lactate Nutrition 0.000 description 1
- 230000003255 anti-acne Effects 0.000 description 1
- 230000000844 anti-bacterial effect Effects 0.000 description 1
- 230000001166 anti-perspirative effect Effects 0.000 description 1
- 230000001153 anti-wrinkle effect Effects 0.000 description 1
- 229940053195 antiepileptics hydantoin derivative Drugs 0.000 description 1
- 239000003213 antiperspirant Substances 0.000 description 1
- 229940027983 antiseptic and disinfectant quaternary ammonium compound Drugs 0.000 description 1
- BTFJIXJJCSYFAL-UHFFFAOYSA-N arachidyl alcohol Natural products CCCCCCCCCCCCCCCCCCCCO BTFJIXJJCSYFAL-UHFFFAOYSA-N 0.000 description 1
- 229960000271 arbutin Drugs 0.000 description 1
- 125000003118 aryl group Chemical group 0.000 description 1
- 239000011668 ascorbic acid Substances 0.000 description 1
- 229960005070 ascorbic acid Drugs 0.000 description 1
- 239000003212 astringent agent Substances 0.000 description 1
- 235000021302 avocado oil Nutrition 0.000 description 1
- 239000008163 avocado oil Substances 0.000 description 1
- RZOBLYBZQXQGFY-HSHFZTNMSA-N azanium;(2r)-2-hydroxypropanoate Chemical compound [NH4+].C[C@@H](O)C([O-])=O RZOBLYBZQXQGFY-HSHFZTNMSA-N 0.000 description 1
- 229960002255 azelaic acid Drugs 0.000 description 1
- 239000003899 bactericide agent Substances 0.000 description 1
- 230000004888 barrier function Effects 0.000 description 1
- 239000011230 binding agent Substances 0.000 description 1
- 238000009835 boiling Methods 0.000 description 1
- 239000006172 buffering agent Substances 0.000 description 1
- DHAZIUXMHRHVMP-UHFFFAOYSA-N butyl tetradecanoate Chemical compound CCCCCCCCCCCCCC(=O)OCCCC DHAZIUXMHRHVMP-UHFFFAOYSA-N 0.000 description 1
- CZBZUDVBLSSABA-UHFFFAOYSA-N butylated hydroxyanisole Chemical compound COC1=CC=C(O)C(C(C)(C)C)=C1.COC1=CC=C(O)C=C1C(C)(C)C CZBZUDVBLSSABA-UHFFFAOYSA-N 0.000 description 1
- BVKZGUZCCUSVTD-UHFFFAOYSA-N carbonic acid Chemical class OC(O)=O BVKZGUZCCUSVTD-UHFFFAOYSA-N 0.000 description 1
- 239000001768 carboxy methyl cellulose Substances 0.000 description 1
- 239000004359 castor oil Substances 0.000 description 1
- 235000019438 castor oil Nutrition 0.000 description 1
- 229960001777 castor oil Drugs 0.000 description 1
- 230000015556 catabolic process Effects 0.000 description 1
- 229960000541 cetyl alcohol Drugs 0.000 description 1
- 229940074979 cetyl palmitate Drugs 0.000 description 1
- 229960005443 chloroxylenol Drugs 0.000 description 1
- 150000001851 cinnamic acid derivatives Chemical class 0.000 description 1
- 150000001860 citric acid derivatives Chemical class 0.000 description 1
- 238000004140 cleaning Methods 0.000 description 1
- AGVAZMGAQJOSFJ-WZHZPDAFSA-M cobalt(2+);[(2r,3s,4r,5s)-5-(5,6-dimethylbenzimidazol-1-yl)-4-hydroxy-2-(hydroxymethyl)oxolan-3-yl] [(2r)-1-[3-[(1r,2r,3r,4z,7s,9z,12s,13s,14z,17s,18s,19r)-2,13,18-tris(2-amino-2-oxoethyl)-7,12,17-tris(3-amino-3-oxopropyl)-3,5,8,8,13,15,18,19-octamethyl-2 Chemical compound [Co+2].N#[C-].[N-]([C@@H]1[C@H](CC(N)=O)[C@@]2(C)CCC(=O)NC[C@@H](C)OP(O)(=O)O[C@H]3[C@H]([C@H](O[C@@H]3CO)N3C4=CC(C)=C(C)C=C4N=C3)O)\C2=C(C)/C([C@H](C\2(C)C)CCC(N)=O)=N/C/2=C\C([C@H]([C@@]/2(CC(N)=O)C)CCC(N)=O)=N\C\2=C(C)/C2=N[C@]1(C)[C@@](C)(CC(N)=O)[C@@H]2CCC(N)=O AGVAZMGAQJOSFJ-WZHZPDAFSA-M 0.000 description 1
- 235000019868 cocoa butter Nutrition 0.000 description 1
- 229940110456 cocoa butter Drugs 0.000 description 1
- 239000003240 coconut oil Substances 0.000 description 1
- 235000019864 coconut oil Nutrition 0.000 description 1
- 239000008119 colloidal silica Substances 0.000 description 1
- 230000000052 comparative effect Effects 0.000 description 1
- 230000003750 conditioning effect Effects 0.000 description 1
- 239000002826 coolant Substances 0.000 description 1
- 229920001577 copolymer Polymers 0.000 description 1
- 239000002285 corn oil Substances 0.000 description 1
- 235000005687 corn oil Nutrition 0.000 description 1
- 235000012343 cottonseed oil Nutrition 0.000 description 1
- 239000002385 cottonseed oil Substances 0.000 description 1
- 229960003624 creatine Drugs 0.000 description 1
- 239000006046 creatine Substances 0.000 description 1
- 229940109239 creatinine Drugs 0.000 description 1
- 238000004132 cross linking Methods 0.000 description 1
- 210000004748 cultured cell Anatomy 0.000 description 1
- KZZKOVLJUKWSKX-UHFFFAOYSA-N cyclobutanamine Chemical compound NC1CCC1 KZZKOVLJUKWSKX-UHFFFAOYSA-N 0.000 description 1
- 238000006731 degradation reaction Methods 0.000 description 1
- 229940124447 delivery agent Drugs 0.000 description 1
- 230000001419 dependent effect Effects 0.000 description 1
- 230000035618 desquamation Effects 0.000 description 1
- 150000001991 dicarboxylic acids Chemical class 0.000 description 1
- 235000015872 dietary supplement Nutrition 0.000 description 1
- 229940028356 diethylene glycol monobutyl ether Drugs 0.000 description 1
- XXJWXESWEXIICW-UHFFFAOYSA-N diethylene glycol monoethyl ether Chemical compound CCOCCOCCO XXJWXESWEXIICW-UHFFFAOYSA-N 0.000 description 1
- 229940075557 diethylene glycol monoethyl ether Drugs 0.000 description 1
- 230000004069 differentiation Effects 0.000 description 1
- 208000010643 digestive system disease Diseases 0.000 description 1
- 239000003085 diluting agent Substances 0.000 description 1
- 229940042399 direct acting antivirals protease inhibitors Drugs 0.000 description 1
- 229960000735 docosanol Drugs 0.000 description 1
- QQQMUBLXDAFBRH-UHFFFAOYSA-N dodecyl 2-hydroxypropanoate Chemical compound CCCCCCCCCCCCOC(=O)C(C)O QQQMUBLXDAFBRH-UHFFFAOYSA-N 0.000 description 1
- 238000001035 drying Methods 0.000 description 1
- 230000000694 effects Effects 0.000 description 1
- 229960002852 ellagic acid Drugs 0.000 description 1
- 235000004132 ellagic acid Nutrition 0.000 description 1
- 238000010828 elution Methods 0.000 description 1
- 239000003623 enhancer Substances 0.000 description 1
- 230000002708 enhancing effect Effects 0.000 description 1
- 210000002615 epidermis Anatomy 0.000 description 1
- 150000002148 esters Chemical class 0.000 description 1
- 150000002170 ethers Chemical class 0.000 description 1
- 238000001704 evaporation Methods 0.000 description 1
- 235000008524 evening primrose extract Nutrition 0.000 description 1
- 239000010475 evening primrose oil Substances 0.000 description 1
- 229940089020 evening primrose oil Drugs 0.000 description 1
- 210000000887 face Anatomy 0.000 description 1
- 239000000796 flavoring agent Substances 0.000 description 1
- 235000019634 flavors Nutrition 0.000 description 1
- 235000013305 food Nutrition 0.000 description 1
- 230000037406 food intake Effects 0.000 description 1
- 239000003205 fragrance Substances 0.000 description 1
- 229910000286 fullers earth Inorganic materials 0.000 description 1
- 230000002538 fungal effect Effects 0.000 description 1
- 208000018685 gastrointestinal system disease Diseases 0.000 description 1
- 239000000174 gluconic acid Substances 0.000 description 1
- 235000012208 gluconic acid Nutrition 0.000 description 1
- 229950006191 gluconic acid Drugs 0.000 description 1
- ZEMPKEQAKRGZGQ-XOQCFJPHSA-N glycerol triricinoleate Natural products CCCCCC[C@@H](O)CC=CCCCCCCCC(=O)OC[C@@H](COC(=O)CCCCCCCC=CC[C@@H](O)CCCCCC)OC(=O)CCCCCCCC=CC[C@H](O)CCCCCC ZEMPKEQAKRGZGQ-XOQCFJPHSA-N 0.000 description 1
- 229960004275 glycolic acid Drugs 0.000 description 1
- 229940094952 green tea extract Drugs 0.000 description 1
- 235000020688 green tea extract Nutrition 0.000 description 1
- 239000003966 growth inhibitor Substances 0.000 description 1
- 230000003779 hair growth Effects 0.000 description 1
- 239000013003 healing agent Substances 0.000 description 1
- PXDJXZJSCPSGGI-UHFFFAOYSA-N hexadecanoic acid hexadecyl ester Natural products CCCCCCCCCCCCCCCCOC(=O)CCCCCCCCCCCCCCC PXDJXZJSCPSGGI-UHFFFAOYSA-N 0.000 description 1
- 229940100463 hexyl laurate Drugs 0.000 description 1
- 150000001469 hydantoins Chemical class 0.000 description 1
- 229930195733 hydrocarbon Natural products 0.000 description 1
- 150000002430 hydrocarbons Chemical class 0.000 description 1
- 239000012052 hydrophilic carrier Substances 0.000 description 1
- 229960004337 hydroquinone Drugs 0.000 description 1
- ZCTXEAQXZGPWFG-UHFFFAOYSA-N imidurea Chemical compound O=C1NC(=O)N(CO)C1NC(=O)NCNC(=O)NC1C(=O)NC(=O)N1CO ZCTXEAQXZGPWFG-UHFFFAOYSA-N 0.000 description 1
- 238000011065 in-situ storage Methods 0.000 description 1
- 238000011534 incubation Methods 0.000 description 1
- 125000000959 isobutyl group Chemical group [H]C([H])([H])C([H])(C([H])([H])[H])C([H])([H])* 0.000 description 1
- 229940078545 isocetyl stearate Drugs 0.000 description 1
- VKPSKYDESGTTFR-UHFFFAOYSA-N isododecane Natural products CC(C)(C)CC(C)CC(C)(C)C VKPSKYDESGTTFR-UHFFFAOYSA-N 0.000 description 1
- 229940093629 isopropyl isostearate Drugs 0.000 description 1
- 229940033357 isopropyl laurate Drugs 0.000 description 1
- 229940074928 isopropyl myristate Drugs 0.000 description 1
- XUGNVMKQXJXZCD-UHFFFAOYSA-N isopropyl palmitate Chemical compound CCCCCCCCCCCCCCCC(=O)OC(C)C XUGNVMKQXJXZCD-UHFFFAOYSA-N 0.000 description 1
- 229940075495 isopropyl palmitate Drugs 0.000 description 1
- 229940089456 isopropyl stearate Drugs 0.000 description 1
- BEJNERDRQOWKJM-UHFFFAOYSA-N kojic acid Chemical compound OCC1=CC(=O)C(O)=CO1 BEJNERDRQOWKJM-UHFFFAOYSA-N 0.000 description 1
- 229960004705 kojic acid Drugs 0.000 description 1
- WZNJWVWKTVETCG-UHFFFAOYSA-N kojic acid Natural products OC(=O)C(N)CN1C=CC(=O)C(O)=C1 WZNJWVWKTVETCG-UHFFFAOYSA-N 0.000 description 1
- 239000004310 lactic acid Substances 0.000 description 1
- 235000014655 lactic acid Nutrition 0.000 description 1
- 235000019388 lanolin Nutrition 0.000 description 1
- 229940039717 lanolin Drugs 0.000 description 1
- 230000007774 longterm Effects 0.000 description 1
- 229940078752 magnesium ascorbyl phosphate Drugs 0.000 description 1
- 239000003550 marker Substances 0.000 description 1
- 239000011159 matrix material Substances 0.000 description 1
- 238000002844 melting Methods 0.000 description 1
- 230000008018 melting Effects 0.000 description 1
- 229940041616 menthol Drugs 0.000 description 1
- 235000010270 methyl p-hydroxybenzoate Nutrition 0.000 description 1
- 239000004292 methyl p-hydroxybenzoate Substances 0.000 description 1
- FAARLWTXUUQFSN-UHFFFAOYSA-N methylellagic acid Natural products O1C(=O)C2=CC(O)=C(O)C3=C2C2=C1C(OC)=C(O)C=C2C(=O)O3 FAARLWTXUUQFSN-UHFFFAOYSA-N 0.000 description 1
- 229960002216 methylparaben Drugs 0.000 description 1
- 239000004530 micro-emulsion Substances 0.000 description 1
- 230000000813 microbial effect Effects 0.000 description 1
- 244000000010 microbial pathogen Species 0.000 description 1
- 239000002480 mineral oil Substances 0.000 description 1
- 235000010446 mineral oil Nutrition 0.000 description 1
- 229940042472 mineral oil Drugs 0.000 description 1
- 238000002156 mixing Methods 0.000 description 1
- 229910052901 montmorillonite Inorganic materials 0.000 description 1
- 229940078812 myristyl myristate Drugs 0.000 description 1
- MNHSXSKBHPGQED-UHFFFAOYSA-N n-cyclobutylpyridine-3-carboxamide Chemical compound C=1C=CN=CC=1C(=O)NC1CCC1 MNHSXSKBHPGQED-UHFFFAOYSA-N 0.000 description 1
- VQRIASKDLZXYTO-UHFFFAOYSA-N n-cyclohexylpyridine-3-carboxamide Chemical compound C=1C=CN=CC=1C(=O)NC1CCCCC1 VQRIASKDLZXYTO-UHFFFAOYSA-N 0.000 description 1
- GOQYKNQRPGWPLP-UHFFFAOYSA-N n-heptadecyl alcohol Natural products CCCCCCCCCCCCCCCCCO GOQYKNQRPGWPLP-UHFFFAOYSA-N 0.000 description 1
- OXGBCSQEKCRCHN-UHFFFAOYSA-N octadecan-2-ol Chemical compound CCCCCCCCCCCCCCCCC(C)O OXGBCSQEKCRCHN-UHFFFAOYSA-N 0.000 description 1
- AEIJTFQOBWATKX-UHFFFAOYSA-N octane-1,2-diol Chemical compound CCCCCCC(O)CO AEIJTFQOBWATKX-UHFFFAOYSA-N 0.000 description 1
- 229940060184 oil ingredients Drugs 0.000 description 1
- 229940055577 oleyl alcohol Drugs 0.000 description 1
- XMLQWXUVTXCDDL-UHFFFAOYSA-N oleyl alcohol Natural products CCCCCCC=CCCCCCCCCCCO XMLQWXUVTXCDDL-UHFFFAOYSA-N 0.000 description 1
- 239000004006 olive oil Substances 0.000 description 1
- 235000008390 olive oil Nutrition 0.000 description 1
- JCGNDDUYTRNOFT-UHFFFAOYSA-N oxolane-2,4-dione Chemical compound O=C1COC(=O)C1 JCGNDDUYTRNOFT-UHFFFAOYSA-N 0.000 description 1
- DXGLGDHPHMLXJC-UHFFFAOYSA-N oxybenzone Chemical compound OC1=CC(OC)=CC=C1C(=O)C1=CC=CC=C1 DXGLGDHPHMLXJC-UHFFFAOYSA-N 0.000 description 1
- BJRNKVDFDLYUGJ-UHFFFAOYSA-N p-hydroxyphenyl beta-D-alloside Natural products OC1C(O)C(O)C(CO)OC1OC1=CC=C(O)C=C1 BJRNKVDFDLYUGJ-UHFFFAOYSA-N 0.000 description 1
- NWVVVBRKAWDGAB-UHFFFAOYSA-N p-methoxyphenol Chemical compound COC1=CC=C(O)C=C1 NWVVVBRKAWDGAB-UHFFFAOYSA-N 0.000 description 1
- 239000003346 palm kernel oil Substances 0.000 description 1
- 235000019865 palm kernel oil Nutrition 0.000 description 1
- 244000045947 parasite Species 0.000 description 1
- 239000002245 particle Substances 0.000 description 1
- 239000000312 peanut oil Substances 0.000 description 1
- 239000000137 peptide hydrolase inhibitor Substances 0.000 description 1
- 239000013503 personal care ingredient Substances 0.000 description 1
- 229940066842 petrolatum Drugs 0.000 description 1
- 235000019271 petrolatum Nutrition 0.000 description 1
- 239000003208 petroleum Substances 0.000 description 1
- XNQULTQRGBXLIA-UHFFFAOYSA-O phosphonic anhydride Chemical compound O[P+](O)=O XNQULTQRGBXLIA-UHFFFAOYSA-O 0.000 description 1
- 229920001495 poly(sodium acrylate) polymer Polymers 0.000 description 1
- 229920000573 polyethylene Polymers 0.000 description 1
- 229920001223 polyethylene glycol Polymers 0.000 description 1
- 229920001451 polypropylene glycol Polymers 0.000 description 1
- XAEFZNCEHLXOMS-UHFFFAOYSA-M potassium benzoate Chemical compound [K+].[O-]C(=O)C1=CC=CC=C1 XAEFZNCEHLXOMS-UHFFFAOYSA-M 0.000 description 1
- 229940114930 potassium stearate Drugs 0.000 description 1
- ANBFRLKBEIFNQU-UHFFFAOYSA-M potassium;octadecanoate Chemical compound [K+].CCCCCCCCCCCCCCCCCC([O-])=O ANBFRLKBEIFNQU-UHFFFAOYSA-M 0.000 description 1
- 102000004196 processed proteins & peptides Human genes 0.000 description 1
- 108090000765 processed proteins & peptides Proteins 0.000 description 1
- XEIOPEQGDSYOIH-MURFETPASA-N propan-2-yl (9z,12z)-octadeca-9,12-dienoate Chemical compound CCCCC\C=C/C\C=C/CCCCCCCC(=O)OC(C)C XEIOPEQGDSYOIH-MURFETPASA-N 0.000 description 1
- NEOZOXKVMDBOSG-UHFFFAOYSA-N propan-2-yl 16-methylheptadecanoate Chemical compound CC(C)CCCCCCCCCCCCCCC(=O)OC(C)C NEOZOXKVMDBOSG-UHFFFAOYSA-N 0.000 description 1
- ZPWFUIUNWDIYCJ-UHFFFAOYSA-N propan-2-yl octadecanoate Chemical compound CCCCCCCCCCCCCCCCCC(=O)OC(C)C ZPWFUIUNWDIYCJ-UHFFFAOYSA-N 0.000 description 1
- 239000003380 propellant Substances 0.000 description 1
- 235000010232 propyl p-hydroxybenzoate Nutrition 0.000 description 1
- 239000004405 propyl p-hydroxybenzoate Substances 0.000 description 1
- 229960003415 propylparaben Drugs 0.000 description 1
- 230000001681 protective effect Effects 0.000 description 1
- RADKZDMFGJYCBB-UHFFFAOYSA-N pyridoxal hydrochloride Natural products CC1=NC=C(CO)C(C=O)=C1O RADKZDMFGJYCBB-UHFFFAOYSA-N 0.000 description 1
- 150000003856 quaternary ammonium compounds Chemical class 0.000 description 1
- 230000005855 radiation Effects 0.000 description 1
- 230000009467 reduction Effects 0.000 description 1
- DOUMFZQKYFQNTF-MRXNPFEDSA-N rosemarinic acid Natural products C([C@H](C(=O)O)OC(=O)C=CC=1C=C(O)C(O)=CC=1)C1=CC=C(O)C(O)=C1 DOUMFZQKYFQNTF-MRXNPFEDSA-N 0.000 description 1
- TVHVQJFBWRLYOD-UHFFFAOYSA-N rosmarinic acid Natural products OC(=O)C(Cc1ccc(O)c(O)c1)OC(=Cc2ccc(O)c(O)c2)C=O TVHVQJFBWRLYOD-UHFFFAOYSA-N 0.000 description 1
- 239000003813 safflower oil Substances 0.000 description 1
- 150000003839 salts Chemical class 0.000 description 1
- 210000002374 sebum Anatomy 0.000 description 1
- 230000008591 skin barrier function Effects 0.000 description 1
- 239000002884 skin cream Substances 0.000 description 1
- 229910052708 sodium Inorganic materials 0.000 description 1
- 235000019812 sodium carboxymethyl cellulose Nutrition 0.000 description 1
- 229920001027 sodium carboxymethylcellulose Polymers 0.000 description 1
- 235000019259 sodium dehydroacetate Nutrition 0.000 description 1
- 229940079839 sodium dehydroacetate Drugs 0.000 description 1
- 239000001540 sodium lactate Substances 0.000 description 1
- 229940005581 sodium lactate Drugs 0.000 description 1
- 235000011088 sodium lactate Nutrition 0.000 description 1
- NNMHYFLPFNGQFZ-UHFFFAOYSA-M sodium polyacrylate Chemical compound [Na+].[O-]C(=O)C=C NNMHYFLPFNGQFZ-UHFFFAOYSA-M 0.000 description 1
- 235000011152 sodium sulphate Nutrition 0.000 description 1
- DSOWAKKSGYUMTF-GZOLSCHFSA-M sodium;(1e)-1-(6-methyl-2,4-dioxopyran-3-ylidene)ethanolate Chemical compound [Na+].C\C([O-])=C1/C(=O)OC(C)=CC1=O DSOWAKKSGYUMTF-GZOLSCHFSA-M 0.000 description 1
- 239000003549 soybean oil Substances 0.000 description 1
- 235000012424 soybean oil Nutrition 0.000 description 1
- 239000007921 spray Substances 0.000 description 1
- 230000000087 stabilizing effect Effects 0.000 description 1
- 239000008107 starch Substances 0.000 description 1
- 235000019698 starch Nutrition 0.000 description 1
- 229960004274 stearic acid Drugs 0.000 description 1
- 230000003637 steroidlike Effects 0.000 description 1
- 235000020238 sunflower seed Nutrition 0.000 description 1
- 230000002195 synergetic effect Effects 0.000 description 1
- 239000000454 talc Substances 0.000 description 1
- 229910052623 talc Inorganic materials 0.000 description 1
- BORJONZPSTVSFP-UHFFFAOYSA-N tetradecyl 2-hydroxypropanoate Chemical compound CCCCCCCCCCCCCCOC(=O)C(C)O BORJONZPSTVSFP-UHFFFAOYSA-N 0.000 description 1
- DZKXJUASMGQEMA-UHFFFAOYSA-N tetradecyl tetradecanoate Chemical compound CCCCCCCCCCCCCCOC(=O)CCCCCCCCCCCCC DZKXJUASMGQEMA-UHFFFAOYSA-N 0.000 description 1
- ICUTUKXCWQYESQ-UHFFFAOYSA-N triclocarban Chemical compound C1=CC(Cl)=CC=C1NC(=O)NC1=CC=C(Cl)C(Cl)=C1 ICUTUKXCWQYESQ-UHFFFAOYSA-N 0.000 description 1
- 229960003500 triclosan Drugs 0.000 description 1
- ZIBGPFATKBEMQZ-UHFFFAOYSA-N triethylene glycol Chemical compound OCCOCCOCCO ZIBGPFATKBEMQZ-UHFFFAOYSA-N 0.000 description 1
- HTJNEBVCZXHBNJ-XCTPRCOBSA-H trimagnesium;(2r)-2-[(1s)-1,2-dihydroxyethyl]-3,4-dihydroxy-2h-furan-5-one;diphosphate Chemical compound [Mg+2].[Mg+2].[Mg+2].[O-]P([O-])([O-])=O.[O-]P([O-])([O-])=O.OC[C@H](O)[C@H]1OC(=O)C(O)=C1O HTJNEBVCZXHBNJ-XCTPRCOBSA-H 0.000 description 1
- 235000015112 vegetable and seed oil Nutrition 0.000 description 1
- 235000019155 vitamin A Nutrition 0.000 description 1
- 239000011719 vitamin A Substances 0.000 description 1
- 235000019163 vitamin B12 Nutrition 0.000 description 1
- 239000011715 vitamin B12 Substances 0.000 description 1
- 235000019158 vitamin B6 Nutrition 0.000 description 1
- 239000011726 vitamin B6 Substances 0.000 description 1
- 235000019154 vitamin C Nutrition 0.000 description 1
- 239000011718 vitamin C Substances 0.000 description 1
- 229940045997 vitamin a Drugs 0.000 description 1
- 229940011671 vitamin b6 Drugs 0.000 description 1
- 150000003722 vitamin derivatives Chemical class 0.000 description 1
- 239000000341 volatile oil Substances 0.000 description 1
- 238000005406 washing Methods 0.000 description 1
- 230000002087 whitening effect Effects 0.000 description 1
- 239000011787 zinc oxide Substances 0.000 description 1
Classifications
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61Q—SPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
- A61Q17/00—Barrier preparations; Preparations brought into direct contact with the skin for affording protection against external influences, e.g. sunlight, X-rays or other harmful rays, corrosive materials, bacteria or insect stings
- A61Q17/005—Antimicrobial preparations
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/455—Nicotinic acids, e.g. niacin; Derivatives thereof, e.g. esters, amides
-
- A—HUMAN NECESSITIES
- A01—AGRICULTURE; FORESTRY; ANIMAL HUSBANDRY; HUNTING; TRAPPING; FISHING
- A01N—PRESERVATION OF BODIES OF HUMANS OR ANIMALS OR PLANTS OR PARTS THEREOF; BIOCIDES, e.g. AS DISINFECTANTS, AS PESTICIDES OR AS HERBICIDES; PEST REPELLANTS OR ATTRACTANTS; PLANT GROWTH REGULATORS
- A01N43/00—Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds
- A01N43/34—Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds having rings with one nitrogen atom as the only ring hetero atom
- A01N43/40—Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds having rings with one nitrogen atom as the only ring hetero atom six-membered rings
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K8/00—Cosmetics or similar toiletry preparations
- A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
- A61K8/30—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
- A61K8/49—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing heterocyclic compounds
- A61K8/4906—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing heterocyclic compounds with one nitrogen as the only hetero atom
- A61K8/4926—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing heterocyclic compounds with one nitrogen as the only hetero atom having six membered rings
Landscapes
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Animal Behavior & Ethology (AREA)
- Public Health (AREA)
- Epidemiology (AREA)
- Agronomy & Crop Science (AREA)
- Zoology (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Environmental Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Pest Control & Pesticides (AREA)
- Plant Pathology (AREA)
- Engineering & Computer Science (AREA)
- Dentistry (AREA)
- Wood Science & Technology (AREA)
- Birds (AREA)
- Dermatology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Cosmetics (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Medicinal Preparation (AREA)
Abstract
本发明涉及一种局部组合物，其包含式(I)的化合物：
Description
发明领域
本发明涉及局部组合物，更特别是涉及用于抗微生物益处的局部组合物。
发明背景
人们通常努力照顾好自己以享受健康的生活方式。通常，这包括照顾他们的外表面，如皮肤、头皮、毛发和口腔。人们努力照顾他们的外表面的一种方式是通过使用递送各种各样益处的局部组合物，如例如无头皮屑的头皮，粗壮浓厚的毛发，没有龋齿、恶臭的口腔，和抗微生物益处，即保持外表面没有微生物，如细菌和一些真菌。
人们面临的许多(如果不是全部)问题都与暴露于微生物如细菌和一些真菌有关。例如，头皮屑与真菌微生物有关。同时，龋齿和恶臭也通常与细菌在口腔中的存在有关。另外，存在常见于人类皮肤的表面上的细菌，如例如大肠杆菌(E.coli)和金黄色葡萄球菌(S.aureus)。虽然这些细菌当存在于皮肤上时不是致病性的，然而如果它们经由摄入进入人体，它们可变成致病性的。
因此，人们通常想要摆脱或至少最少化暴露于有害或可变得有害的微生物。人们努力获得这一点的一种方式是通过在感染已经来临之后施用抗微生物化合物。而另一种方式是将很小量的诱导生成抗微生物肽(AMP)(如例如来自皮肤的牛皮癣素)的化合物留在外表面上，如例如皮肤上。
AMP构成皮肤的自身防御系统的不可或缺的部分。AMP最初是在昆虫和动物中发现的，并且从其最初被发现时开始AMP就被认为是有前景的抗微生物剂。AMP在自然界中无处不在，并且其通常表现出广谱的对抗侵入性细菌、真菌、包膜病毒和寄生虫的活性(Braff和Gallo,2006)。AMP通常是短肽，并且据报道在人类中存在约90种不同的AMP。
描述用于生成AMP的化合物如烟酰胺的一些参考文献见于现有技术中。
WO 2015/172801(Unilever,2015)公开了烟酰胺用于触发在皮肤上产生AMP的新用途。这具有在改善皮肤、头皮和口腔对抗微生物的攻击的免疫力方面的应用。
尽管存在技术，但是人们通常展望将通过生成AMP来递送改善的抗微生物益处，从而改善皮肤、头皮和口腔的免疫力的新技术。
因此，需要提供新技术，如例如通过AMP生成而提供改善的抗微生物益处的化合物和包含这样的化合物的局部组合物。
因此，本发明的一个目的是提供包含当施用到人类皮肤上时通过AMP生成而提供改善的抗微生物益处的化合物的局部组合物。
已经发现式I的化合物当施用到人类皮肤时通过AMP生成提供抗微生物益处，由此满足上述目的中的一个或多个。
发明内容
在第一方面，本发明涉及一种局部组合物，其包含0.001至10重量％的式I的化合物，
其中R为环烷基中的碳原子总数在4至6范围内的环烷基。
在第二方面，本发明涉及一种消毒表面的方法，其包括将第一方面的组合物施用到所述表面上的步骤，其中所述表面为人体的外表面。
在第三方面，本发明涉及第一方面的组合物用于当施用到人体的外表面上时获得抗微生物益处的用途。
在第四方面，本发明涉及第一方面的组合物用于当施用到人体的外表面上时诱导AMP生成的用途。
在第五方面，本发明涉及式I的化合物用于当施用到人体的外表面上时获得抗微生物益处的用途，
其中R为环烷基中的碳原子总数在4至6范围内的环烷基。
本发明的一个方面的任何特征可用于本发明的任何其它方面。词语“包含”旨在表示“包括”，但不一定是“由...组成”或“由...构成”。换句话说，所列步骤或选项不需要是穷举性的。除非是在操作和比较实施例中，或在另外明确指出的情况下，否则本说明书中指示材料的量或反应条件、材料的物理特性和/或用途的所有数字均应理解为由词语“约”修饰。以“x至y”格式表示的数字范围应理解为包括x和y。当针对特定特征以“x至y”格式描述多个优选范围时，应当理解还预期组合不同端点的所有范围。
具体实施方式
在第一方面，本发明涉及一种局部组合物，其包含式I的化合物：
其中R为环烷基中的碳原子总数在4至6范围内的环烷基。
式I的化合物的实例包括其中环烷基中的碳原子总数为下述的化合物：
-4，即N-环丁基尼克酰胺，
-5，即N-环戊基尼克酰胺；和
-6，即N-环己基尼克酰胺。
优选的式I的化合物为上述提及的三种化合物中的任一种。更优选的式I的化合物为其中环烷基中的碳原子数为5的，即N-环戊基尼克酰胺。
组合物包含按重量计0.001至10％、优选0.002至8％、更优选0.005至8％、甚至更优选0.01至6％、仍然更优选0.05至5％，还更优选0.1至4％，进一步更优选0.5至3％，最优选1至1.5％的式I的化合物。
优选地，组合物进一步包含选自烟酰胺、吡啶酰胺和异尼克酰胺的至少一种成分。优选地，所述成分是烟酰胺。
烟酰胺，也称为尼克酰胺，是烟酸的酰胺形式。其是见于食品中的维生素。其也用作食品补充剂。烟酰胺具有以下化学结构：
吡啶酰胺和异烟酰胺是烟酰胺的异构体，具有以下结构：
当存在时，组合物包含0.001至10％，优选0.005至8％，更优选0.01至6％，甚至更优选0.05至5％，进一步更优选0.1至4％，还更优选0.5至3％和仍然更优选1至1.5％的烟酰胺或吡啶酰胺或异尼克酰胺。
如果同时存在这三种化合物中的多于一种，则组合物中可以包含的这些化合物的总量按重量计在0.001至10％，优选0.005至8％，更优选0.01至6％，甚至更优选0.05至5％，进一步更优选0.1至4％，还更优选0.5至3％和仍然更优选1至1.5％的范围内。
用于合成式I的化合物的优选方案：
首先，在无水二氯甲烷(DCM)中制备烟酸溶液。在惰性气氛下，在0℃下，将丙基膦酸酐(T3P，在乙醇中)、三乙醇胺(TEA)和环烷胺加入该溶液中。所述环烷胺可选自环丁胺、环戊胺和环己胺。最优选的是环戊胺。然后在约25℃下搅拌该反应混合物6至24小时，更优选8至20小时，最优选10至14小时。在如优选地通过薄层色谱法(TLC)监测反应完成之后，将反应物质优选地分配在DCM和水之间。然后分离各层，并再次在10％甲醇和/或DCM中萃取水层。然后用水、盐水溶液洗涤合并的萃取物，并经Na2SO4干燥。然后将溶剂蒸发到干燥。最后纯化粗产物以获得纯的式1的化合物。
组合物优选进一步包含化妆品可接受的基质。所述化妆品可接受的基质优选为乳霜、洗液、凝胶或乳液的形式。
可以使用不同的化妆品可接受的乳化或非乳化基质制备组合物。一种高度合适的基质是乳霜。雪花膏(vanishing cream)是特别优选的。雪花膏基质通常包含脂肪酸和皂的混合物。雪花膏基质赋予皮肤高度受关注的哑光感(matty feel)。在雪花膏基质中，C12至C20脂肪酸是特别优选的，进一步更优选的是C14至C18脂肪酸。最优选地，脂肪酸为硬脂酸或棕榈酸或其混合物。脂肪酸通常为hystric acid，其基本上为(通常90至95重量％)45％硬脂酸和55％棕榈酸的混合物。因此，包含hystric acid及其皂以制备本发明的组合物是在本发明的范围内。组合物中的脂肪酸按组合物的重量计优选以5至20％，更优选6至19％和甚至更优选7至17％的量存在。雪花膏基质中的皂包括脂肪酸的碱金属盐，如钠盐或钾盐，最优选的是硬脂酸钾。雪花膏基质中的皂通常以组合物的0.1至10重量％，更优选0.1至3重量％的量存在。通常，雪花膏基质局部组合物通过取期望量的总脂肪物质并与期望量的氢氧化钾混合来制备。皂通常在混合过程中原位形成。
特别合适的化妆品可接受的基质是包含油包水乳液的基质，所述油包水乳液包含硅油作为连续相。油包水乳液优选包含交联的硅酮弹性体共混物。
将硅酮弹性体共混物包含在油包水乳液中可以用作制备本发明组合物的化妆品可接受的基质。虽然可以使用硅酮流体，但是特别优选交联的硅酮弹性体。与硅酮流体聚合物相比，弹性体的物理性质通常取决于交联的数量，而不是分子量。硅酮弹性体溶胀的能力使其成为油相的理想增稠剂。当施用于皮肤或毛发时，弹性体具有非常光滑和柔软的感觉。它们还可以用作化妆品组合物中的香味剂、维生素和其他添加剂的递送剂。可商购且适合包含在本发明的组合物中且发现提供增强的稳定性的合适的硅酮弹性体共混物或凝胶是：Dow
EL-8051IN硅酮有机弹性体共混物[INCI名：新戊酸异癸酯(和)二甲聚硅氧烷/双异丁基PPG-20交联聚合物]；EL-8050[INCI名：异十二烷(和)二甲聚硅氧烷/双异丁基PPG 20交联聚合物]；DC9040，DC9041，DC9045(二甲聚硅氧烷交联聚合物)；DC9506，DC9509(二甲聚硅氧烷乙烯基二甲聚硅氧烷交联聚合物)；和Shin-Etsu KSG-15，KSG-16，KSG-17(二甲聚硅氧烷乙烯基二甲聚硅氧烷交联聚合物)。进一步优选的是，组合物包含5至50重量％的硅酮弹性体。
也可以使用水和/或醇作为化妆品可接受的基质。醇可以是一元醇或多元醇。一元醇通常是短链，其意味着它们含有至多6个碳，实际上，最常见是乙醇或有时是异丙醇。多元醇通常包括乙二醇或丙二醇，或者可以使用同系物如二甘醇。
化妆品可接受的基质通常按组合物的重量计为10至99.9％，优选50至99％。
优选地，组合物进一步包含亮肤剂。在组合物中可以使用的亮肤剂的实例包括12-羟基硬脂酸、芦荟提取物、乳酸铵、熊果苷、壬二酸、曲酸、丁基羟基茴香醚、丁基羟基甲苯、柠檬酸酯、3-二苯基丙烷衍生物、2,5-二羟基苯甲酸及其衍生物、鞣花酸、茴香提取物、吡喃葡糖基-1-抗坏血酸、葡萄糖酸、乙醇酸、绿茶提取物、氢醌、4-羟基茴香醚及其衍生物、4-羟基苯甲酸衍生物、羟基辛酸、柠檬提取物、亚油酸、磷酸抗坏血酸酯镁、桑树根提取物、2,4-间苯二酚衍生物、3,5-间苯二酚衍生物、水杨酸、维生素(如维生素B6、维生素B12、维生素C、维生素A)、二羧酸、间苯二酚衍生物、羟基羧酸(如乳酸)及其盐(如乳酸钠)、及其混合物。
优选地，组合物进一步包含一种或多种防晒剂。可以加入可以适合地与基质一起使用的任何防晒剂。可以优选地加入UVA和UVB防晒剂两者。
本发明的组合物可以优选地包含UV-A防晒剂，其是二苯甲酰甲烷或其衍生物。优选的二苯甲酰甲烷衍生物选自4-叔丁基-4'-甲氧基二苯甲酰甲烷、2-甲基二苯甲酰甲烷、4-甲基-二苯甲酰甲烷、4-异丙基二苯甲酰甲烷、4-叔丁基二苯甲酰甲烷、2,4-二甲基二苯甲酰甲烷、2,5-二甲基二苯甲酰甲烷、4,4'-二异丙基-二苯甲酰甲烷、2-甲基-5-异丙基-4'-甲氧基二苯甲酰甲烷、2-甲基-5-叔丁基-4'-甲氧基-二苯甲酰甲烷、2,4-二甲基-4'-甲氧基二苯甲酰甲烷或2,6-二甲基-4-叔丁基-4'-甲氧基-二苯甲酰甲烷。最优选的二苯甲酰甲烷衍生物是4-叔丁基-4'-甲氧基二苯甲酰甲烷。本发明的组合物优选地包含基于组合物的总重量0.1至10重量％，更优选0.2至5重量％，还更优选0.4至3重量％的二苯甲酰甲烷或其衍生物，并且包括其中包括的所有范围。
组合物也可以优选地包含选自肉桂酸、水杨酸、二苯基丙烯酸及其衍生物的种类的UV-B有机防晒剂。可商购且可用于包含在本发明的组合物中的UV-B防晒剂的说明性非限制性实例是奥替柳酯TM、胡莫柳酯TM、NeoHelipanTM、奥克立林TM、氧苯酮TM或Parsol MCXTM。UV-B防晒剂最优选是2-乙基-己基-4-甲氧基肉桂酸酯，其可作为Parsol MCXTM商购。UV-B有机防晒剂优选地以组合物的0.1至10重量％，更优选0.1至7重量％包含在组合物中。已经观察到有机UV-B防晒剂如2-乙基-己基-4-甲氧基肉桂酸酯的存在导致在紫外线辐射存在下UV-A二苯甲酰甲烷防晒剂进一步快速降解。发现迷迭香酸酯化合物的存在即使在存在UV-B防晒剂时也在使组合物稳定化方面非常有效。
可用的无机防晒霜(sun-block)也优选地用于本发明中。这些包括例如氧化锌、氧化铁、二氧化硅(如热解二氧化硅)和二氧化钛。
组合物可以进一步包含防腐剂以使免于潜在有害微生物的生长。适用于本发明的组合物的传统防腐剂是对羟基苯甲酸的烷基酯。最近已经开始使用的其他防腐剂包括乙内酰脲衍生物、丙酸盐和各种季铵化合物。特别优选的防腐剂是苯氧乙醇、尼泊金甲酯、尼泊金丙酯、咪唑烷基脲、脱氢乙酸钠、苄醇、烷二醇，最优选1,2-辛二醇和苯氧乙醇。应当考虑组合物的用途和防腐剂与其他成分之间可能的不相容性而选择防腐剂。防腐剂优选地以组合物的0.01重量％至2重量％的量使用。
可以将各种其他任选材料配制到组合物中。这些可以包括：抗微生物剂，如2-羟基-4,2',4'-三氯二苯醚(三氯生)、2,6-二甲基-4-羟基氯苯、和3,4,4'-三氯碳酸替苯胺；磨砂和去角质颗粒，如聚乙烯和二氧化硅或氧化铝；清凉剂，如薄荷醇；皮肤舒缓剂，如芦荟；和着色剂。
此外，组合物可以还包含0至10重量％的遮光剂和珠光剂，如二硬脂酸乙二醇酯、二氧化钛或
621(苯乙烯/丙烯酸酯共聚物)；其均可用于增强产品的外观或性质。
组合物中可以使用的除水以外的稀释剂可以包括液体或固体润肤剂、溶剂、湿润剂、增稠剂和粉剂。这些类型的载体各自的实例，其可以单独或者作为一种或多种载体的混合物使用，如下：
优选地，组合物包含润肤剂。可以存在的润肤剂的实例包括硬脂醇、单蓖麻油酸甘油酯、貂油、鲸蜡醇、异硬脂酸异丙酯、硬脂酸、棕榈酸异丁酯、硬脂酸异鲸蜡酯、油醇、月桂酸异丙酯、月桂酸己酯、油酸癸酯、十八烷-2-醇、异鲸蜡醇、二十烷醇、山嵛醇、棕榈酸鲸蜡酯、硅油(如二甲基聚硅氧烷)、癸二酸二正丁酯、肉豆蔻酸异丙酯、棕榈酸异丙酯、硬脂酸异丙酯、硬脂酸丁酯、聚乙二醇、三甘醇、羊毛脂、可可脂、玉米油、棉籽油、橄榄油、棕榈仁油、菜籽油、红花籽油、月见草油、豆油、葵花籽油、鳄梨油、芝麻籽油、椰子油、花生油、蓖麻油、乙酰化羊毛脂醇、凡士林、矿物油、肉豆蔻酸丁酯、异硬脂酸、棕榈酸、亚油酸异丙酯、乳酸月桂酯、乳酸肉豆蔻酯、油酸癸酯、肉豆蔻酸肉豆蔻酯。
优选地，组合物包含溶剂，如乙醇、异丙醇、丙酮、乙二醇单乙醚、二甘醇单丁醚、二甘醇单乙醚及其混合物。
有利地，组合物可以优选地包含成分如杀细菌剂、维生素、抗痤疮活性物质；抗皱、抗皮肤萎缩和皮肤修复活性物质、皮肤屏障修复活性物质、非甾体化妆品舒缓活性物质、人工晒黑剂和加速剂、皮脂刺激剂、皮脂抑制剂、抗氧化剂、蛋白酶抑制剂、紧肤剂、止痒成分、毛发生长抑制剂、5-α还原酶抑制剂、脱皮酶增强剂、抗糖化剂、及其混合物。
组合物可以优选地包含粉末，如例如白垩、滑石、漂白土、高岭土、淀粉、树胶、胶体二氧化硅、聚丙烯酸钠、四烷基和/或三烷基芳基铵蒙脱石、化学改性的硅酸镁铝、有机改性的蒙脱石粘土、水合硅酸铝、热解二氧化硅、羧乙烯基聚合物、羧甲基纤维素钠、单硬脂酸乙二醇酯、及其混合物。
本发明的组合物可以包含宽范围的其他任选组分。CTFA个人护理成分手册(CTFAPersonal Care Ingredient Handbook，第2版，1992)，其全部内容通过引入并入本文，描述了在皮肤护理工业中常用的各种各样的非限制性的个人护理和药物成分，其适于在本发明的组合物中使用。实例包括：抗氧化剂、粘合剂、生物添加剂、缓冲剂、着色剂、增稠剂、聚合物、收敛剂、香味剂、湿润剂、遮光剂、调理剂、pH调节剂、天然提取物、精油、皮肤感觉剂、皮肤舒缓剂和皮肤愈合剂。
组合物也可包含以下成分中的一种或多种：例如苄索氯铵(BEC)、苯扎氯铵(BKC)、氯二甲苯酚、吡啶硫酮锌(ZPT)、肌酸和肌酸酐。
组合物优选为洗去型或免洗型组合物的形式，优选免洗型组合物。
洗去型组合物优选是指旨在/需要在施用组合物如例如洗手组合物和洗脸组合物之后，通过用溶剂(优选水)洗涤而从身体除去的组合物。
免洗组合物优选是指不需要在施用组合物如例如护肤霜、润肤液、手消毒剂(handsanitizer)和除臭剂之后从人体除去的组合物。
当组合物为免洗型组合物的形式时，该组合物可以为除臭剂、手消毒剂、洗剂、乳霜和身体喷雾剂的形式。
本发明的组合物可以优选包含常规除臭剂基质作为化妆品可接受的载体。除臭剂是指可以用于个人除臭益处(例如，在腋下区域施用)的在棒状的、滚抹的或推进剂介质中的产品，其可以含有或可以不含有止汗剂活性物质。
除臭剂组合物通常可以是硬固体、软固体、凝胶、霜剂和液体的形式，并且使用适于组合物的物理特性的施用器分配。通过滚抹递送的除臭剂组合物通常包含液体载体。这样的液体载体可以是疏水性的或者包含亲水性和疏水性液体两者的混合物。它们可以是乳液或微乳液的形式。液体载体或载体混合物通常构成组合物的30至95重量％，并且在很多情况下40至80重量％。疏水性液体载体通常可以包含选自以下化学类别中的一种或多种材料：具有不超过25℃的熔点和至少100℃的沸点的硅氧烷、烃、支链脂族醇、酯和醚。可用于本文的组合物中的亲水性载体液体通常包括水和/或一元或多元醇或水可混溶同系物。一元醇通常是短链，这意味着其含有至多6个碳，并且实践中最常见是乙醇或有时是异丙醇。多元醇通常包括乙二醇或丙二醇，或可使用同系物如二甘醇。除此之外，可以加入适用于除臭剂组合物的其他载体和组分。
当组合物是手消毒剂的形式时，化妆品可接受的基质可以包括醇和水。最优选的醇是乙醇和异丙醇。甚至两种或更多种醇的混合物也可优选地用于手消毒剂组合物中。醇的量优选为手消毒剂组合物的50至95重量％，更优选60至80重量％，最优选65至80重量％。
在第二方面，本发明还提供了清洁或消毒表面的方法，其在免洗型组合物的情况下包括施用第一方面的组合物的步骤，其中所述表面是人体的外表面。如果组合物是洗去型组合物的形式，则该方法任选地包括从表面至少部分地除去组合物的另外的步骤。优选地，至少部分除去组合物的步骤在将组合物施用到人体的外表面上的步骤之后的不到5分钟内进行。优选地，方法是非治疗性的。
在第三方面，本发明进一步提供第一方面的组合物用于在施用到人体的外表面上时获得抗微生物益处的用途。抗微生物益处优选是指杀死或至少引起常见致病性微生物大量减少的能力。常见致病性革兰氏阳性生物包括葡萄球菌属(Staphylococcus spp.)、链球菌属(Streptococcus spp.)和肠球菌属(Enterococcus spp.)。常见致病性革兰氏阴性生物中的一些包括大肠杆菌、沙门氏菌属、克雷伯氏菌属和志贺氏菌属。大肠杆菌和沙门氏菌属可引起严重的胃肠疾病。本发明的组合物提供在施用到人体的外表面上时改善的抗微生物益处。
本发明的组合物提供长期/持久的抗微生物益处。
在第四方面，本发明还提供第一方面的组合物用于当施用到人体的外表面上时诱导生成AMP的用途。
在第五方面，本发明还提供式I的化合物用于当施用到人体的外表面上时获得抗微生物益处的用途，
其中R为环烷基中的碳原子总数在4至6范围内的环烷基。
人体的外表面包括皮肤、头皮、毛发和口腔。
已经发现通过本发明，式I的化合物激活角化细胞(其是皮肤表皮中的主要细胞)以提供本发明的益处，即诱导分泌AMP。这导致增强了对抗微生物的保护屏障。因此包含式I的化合物的组合物通过增强身体自身的防御而为身体提供了对抗感染的保护。换句话说，式I的化合物使身体表面准备好微生物保护。这个的优势是使得其提供了对抗微生物的持久保护(例如，至多24小时的保护)。
本发明的组合物的用途可以优选地是用于手部卫生。
组合物的预期用途可以用于治疗性或非治疗性目的。然而，本发明的组合物的优选预期用途是非治疗性的和/或美容性的。
本发明还提供了式I的化合物与选自烟酰胺、吡啶酰胺和异尼克酰胺的至少一种化合物的组合用于诱导生成AMP的用途。有关本发明的组合物的优选项同样适用于根据本发明的用途。
现将通过以下非限制性实施例示范本发明。
实施例
实施例1：其中环烷基中的碳原子总数为5的式I的化合物(即，N-环戊基尼克酰胺)
的合成
材料：
烟酸(sigma目录号C115002)，丙基膦酸酐(T3P；Aldrich，目录号87801)，二氯甲烷无水物(DCM；Sigma，目录号270997)，三乙醇胺，乙酸乙酯，甲醇，硫酸钠无水物()。
实验程序：
在惰性气氛下，在0℃下，向烟酸(1g，8.12mmol，1当量)在无水DCM(10vol)中的搅拌溶液中加入丙基膦酸酐(T3P)(3.87g，在EtOAc中的50％溶液，12.18mmol，1.5当量)、TEA(2.46g，24.3mmol，3当量)和环戊胺(0.76g，8.93mmol，1.1当量)。然后在约25℃下搅拌反应混合物约12小时。在如通过薄层色谱法(TLC)监测反应完成之后，将反应物质分配在DCM和水之间。分离层，并再次在10％MeOH/DCM中萃取水层。将合并的提取物用水、盐水溶液洗涤，并干燥(Na2SO4)。将溶剂蒸发到干燥；通过用在石油醚(pet ether)中的50％乙酸乙酯进行Biotage Isolera洗脱来纯化粗产物以提供作为无色粘稠液体(1.15g，产率75％)的最终化合物，纯度为97.72％。
展示在存在或不存在烟酰胺的情况下，用N-环戊基尼克酰胺，即式I的化合物处理 之后，人角质形成细胞生成牛皮癣素(一种抗微生物肽)的体外实验：使用以下方案进行该实验：
步骤1：人新生儿原代皮肤角质形成细胞(NHEK)细胞获自
使用传代3至4次的上述细胞进行该实验。然后将细胞接种(35,000个细胞/孔)在含有获自
的角质形成细胞生长培养基(KGM)的24孔板中。随后将板在37±2℃下，在CO2培养箱中培养48小时。
步骤2：培养48小时之后，通过将培养基更换为补充有2mM氯化钙溶液的新鲜KGM，而诱导细胞分化。接着，在37±2℃下，在CO2培养箱中培养48小时。
步骤3：随后，采用补充有2mM氯化钙溶液的角质形成细胞生长培养基，用不同浓度(如下表1所列)的N-环戊基尼克酰胺处理细胞。
表1：
步骤4：在上述处理之后，将细胞再次在37±2℃下，在CO2培养箱中培养72小时。
步骤5：在培养72小时之后，将来自每个孔的细胞培养物上清液收集在无菌管中。然后，将样品储存在-80℃下，直至用于使用获自
的牛皮癣素ELISA试剂盒(编号：CY-8073)，通过标准ELISA技术测试牛皮癣素分泌。在目前的实验中，将牛皮癣素用作AMP的标记物。
步骤6：通过使用来自每个样品的100μL细胞培养物上清液，实施ELISA方法。
数据按照超过对照(没有处理：实施例A)的倍数变化表示。将在对照(实施例A)的情况下牛皮癣素水平的倍数变化当作等于1倍。在所有其它实施例中列出的由于处理而获得的牛皮癣素的任何倍数变化都超过且高于从对照获得的1倍变化。例如，实施例C显示倍数变化为1.4倍，其是指0.4倍超过且高于从对照获得的1倍。同样，实施例5显示倍数变化为2.84，其是指1.84倍超过且高于从对照获得的1倍。
结果总结在下表2中：
表2：
| 实施例 | 倍数变化 |
| A | 1 |
| B | 0.9 |
| C | 1.4 |
| 1 | <u>2.06</u> |
| 2 | <u>2.84</u> |
从上表明显的是，当与对照相比时，N-环戊基尼克酰胺在牛皮癣素生成方面提供好得多的倍数变化。当以相同浓度，即200μg/mL使用时，N-环戊基尼克酰胺(实施例1)提供与烟酰胺(实施例B)相比好得多的牛皮癣素的倍数变化。当N-环戊基尼克酰胺以一定浓度，即400μg/mL使用时(实施例2)，其提供高达2.84的牛皮癣素的倍数变化。另一方面，更高浓度的烟酰胺，即500μg/mL(实施例C)显示等于仅1.4的倍数变化。因此，N-环戊基尼克酰胺提供改善的AMP生成，由此提供改善的抗微生物益处。
总之，在与对照(没有处理)相比和与已知化合物如例如烟酰胺对AMP的生成相比时，式I的化合物在施用到人类皮肤时通过AMP生成提供改善的抗微生物益处。并且，式I的化合物与选自烟酰胺、吡啶酰胺、异尼克酰胺及其混合物的化合物的组合提供AMP的协同生成。
Claims (13)
1.一种局部组合物，其包含0.001至10重量％的式I的化合物，
其中R为环烷基中的碳原子总数在4至6范围内的环烷基。
2.根据权利要求1所述的局部组合物，其中所述环烷基中的碳原子总数为5。
3.如权利要求1或2所述的局部组合物，其进一步包含0.001至10重量％的选自烟酰胺、吡啶酰胺和异尼克酰胺的至少一种成分。
4.如权利要求3所述的局部组合物，其中所述成分为烟酰胺。
5.如权利要求1至4中任一项所述的组合物，其进一步包含化妆品可接受的基质。
6.如权利要求1至5中任一项所述的组合物，其中所述组合物为洗去型组合物的形式。
7.如权利要求1至5中任一项所述的组合物，其中所述组合物为免洗型组合物的形式。
8.一种消毒表面的方法，其包括将如权利要求1至7中任一项所述的组合物施用到所述表面上的步骤，其中所述表面是人体的外表面。
9.如权利要求8所述的方法，其中所述组合物为洗去型组合物的形式，并且其中所述方法包括至少部分除去所述组合物的附加步骤。
10.如权利要求9所述的方法，其中至少部分除去所述组合物的所述步骤在将所述组合物施用到所述人体的外表面上的所述步骤之后不到5分钟内进行。
11.如权利要求1至7中任一项所述的组合物用于当施用到人体的外表面上时获得抗微生物益处的用途。
12.如权利要求1至7中任一项所述的组合物用于当施用到人体的外表面上时诱导分泌抗微生物肽(AMP)的用途。
13.式1的化合物用于当施用到人体的外表面上时获得抗微生物益处的用途，
其中R为环烷基中的碳原子总数在4至6范围内的环烷基。
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP17208131 | 2017-12-18 | ||
| EP17208131.7 | 2017-12-18 | ||
| PCT/EP2018/085269 WO2019121548A1 (en) | 2017-12-18 | 2018-12-17 | A topical composition based on niacinamide derivative |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CN111683649A true CN111683649A (zh) | 2020-09-18 |
Family
ID=60673832
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201880081650.XA Pending CN111683649A (zh) | 2017-12-18 | 2018-12-17 | 基于烟酰胺衍生物的局部组合物 |
Country Status (6)
| Country | Link |
|---|---|
| US (1) | US20200316050A1 (zh) |
| EP (1) | EP3727316B1 (zh) |
| CN (1) | CN111683649A (zh) |
| BR (1) | BR112020010720B1 (zh) |
| MX (1) | MX2020006280A (zh) |
| WO (1) | WO2019121548A1 (zh) |
Families Citing this family (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP4398869A1 (en) | 2021-09-06 | 2024-07-17 | Unilever IP Holdings B.V. | A deodorant composition |
| WO2023119230A1 (en) | 2021-12-22 | 2023-06-29 | L'oreal | Coagulation pathway and nicotinamide-adenine dinucleotide pathway modulating compositions and methods of their use |
| WO2024041910A1 (en) * | 2022-08-25 | 2024-02-29 | Unilever Ip Holdings B.V. | Inactivation or kill of virus and compositions thereof |
Citations (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US3464998A (en) * | 1968-03-04 | 1969-09-02 | Searle & Co | Adamantyl esters and amides of pyridinecarboxylic acids |
| US3822277A (en) * | 1967-11-13 | 1974-07-02 | C Dufour | Certain pyridyl cyclopropylamides |
| US20010049382A1 (en) * | 2000-04-14 | 2001-12-06 | Jacobson Elaine L. | Topical formulations for the transdermal delivery of niacin and methods of treating hyperlipidemia |
| US20110123510A1 (en) * | 2009-09-24 | 2011-05-26 | Washington University | Methods of Affecting Biological Function Through Circadian Clock Feedback Cycle by NAMPT-Mediated NAD+ Biosynthesis |
| WO2015172801A1 (en) * | 2014-05-12 | 2015-11-19 | Unilever N.V. | Niacinamide for inducing generation of antimicrobial peptides |
Family Cites Families (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN113242751B (zh) * | 2018-12-18 | 2023-09-19 | 联合利华知识产权控股有限公司 | 抗微生物组合物 |
-
2018
- 2018-12-17 CN CN201880081650.XA patent/CN111683649A/zh active Pending
- 2018-12-17 EP EP18825653.1A patent/EP3727316B1/en active Active
- 2018-12-17 WO PCT/EP2018/085269 patent/WO2019121548A1/en active Search and Examination
- 2018-12-17 BR BR112020010720-4A patent/BR112020010720B1/pt active IP Right Grant
- 2018-12-17 MX MX2020006280A patent/MX2020006280A/es unknown
- 2018-12-17 US US16/766,834 patent/US20200316050A1/en not_active Abandoned
Patent Citations (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US3822277A (en) * | 1967-11-13 | 1974-07-02 | C Dufour | Certain pyridyl cyclopropylamides |
| US3464998A (en) * | 1968-03-04 | 1969-09-02 | Searle & Co | Adamantyl esters and amides of pyridinecarboxylic acids |
| US20010049382A1 (en) * | 2000-04-14 | 2001-12-06 | Jacobson Elaine L. | Topical formulations for the transdermal delivery of niacin and methods of treating hyperlipidemia |
| US20110123510A1 (en) * | 2009-09-24 | 2011-05-26 | Washington University | Methods of Affecting Biological Function Through Circadian Clock Feedback Cycle by NAMPT-Mediated NAD+ Biosynthesis |
| WO2015172801A1 (en) * | 2014-05-12 | 2015-11-19 | Unilever N.V. | Niacinamide for inducing generation of antimicrobial peptides |
| CN106413680A (zh) * | 2014-05-12 | 2017-02-15 | 荷兰联合利华有限公司 | 用于诱导抗微生物肽生成的烟酰胺 |
Non-Patent Citations (2)
| Title |
|---|
| LUCILLE等: "STUDIES ON NICOTINAMIDE DERIVATIVES" * |
| LUCILLE等: "STUDIES ON NICOTINAMIDE DERIVATIVES", 《JOURNAL OF BACTERIOLOGY, AMERICAN SOCIETY FOR MICROBIOLOGY》 * |
Also Published As
| Publication number | Publication date |
|---|---|
| MX2020006280A (es) | 2021-11-12 |
| WO2019121548A1 (en) | 2019-06-27 |
| US20200316050A1 (en) | 2020-10-08 |
| EP3727316A1 (en) | 2020-10-28 |
| BR112020010720A2 (pt) | 2020-11-10 |
| EP3727316B1 (en) | 2021-10-13 |
| BR112020010720B1 (pt) | 2023-11-14 |
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| CN108135824B (zh) | 包含烟酰胺和吡啶2-甲酰胺的组合物 | |
| EP3727316B1 (en) | A topical composition based on niacinamide derivative | |
| CN113242751B (zh) | 抗微生物组合物 | |
| CN109069375B (zh) | 包含百里酚、萜品醇和阳离子磷脂的抗微生物组合物 | |
| EP3727315B1 (en) | A topical composition comprising n-cyclopropyl nicotinamide | |
| CN111491510A (zh) | 抗微生物组合物 | |
| CN111491606A (zh) | 抗微生物组合物 | |
| BR112020011640B1 (pt) | Composição tópica e usos não terapêuticos da composição | |
| EA036416B1 (ru) | Противомикробная композиция | |
| BR112020010392B1 (pt) | Composição antimicrobiana, método não terapêutico para limpeza ou desinfecção de uma superfície, uso não terapêutico de uma composição e usos de uma composição |
Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| PB01 | Publication | ||
| PB01 | Publication | ||
| SE01 | Entry into force of request for substantive examination | ||
| SE01 | Entry into force of request for substantive examination | ||
| TA01 | Transfer of patent application right |
Effective date of registration: 20210802 Address after: Rotterdam Applicant after: Unilever Intellectual Property Holdings Ltd. Address before: Rotterdam Applicant before: Netherlands Unilever Co.,Ltd. |
|
| TA01 | Transfer of patent application right |