UA112667C2 - Комбінація антагоніста crth2 і інгібітору протонного насоса для лікування еозинофільного езофагіту - Google Patents

Info

Publication number

UA112667C2

UA112667C2 UAA201407393A UAA201407393A UA112667C2 UA 112667 C2 UA112667 C2 UA 112667C2 UA A201407393 A UAA201407393 A UA A201407393A UA A201407393 A UAA201407393 A UA A201407393A UA 112667 C2 UA112667 C2 UA 112667C2

Authority

UA

Ukraine

Prior art keywords

methyl

acetic acid

fluoro

indol

methylindol

Prior art date

2011-12-16

Links

• Espacenet
• Global Dossier
• Discuss

• 206010064212 Eosinophilic oesophagitis Diseases 0.000 title claims abstract description 40
• 201000000708 eosinophilic esophagitis Diseases 0.000 title claims abstract description 40
• 229940126409 proton pump inhibitor Drugs 0.000 title claims abstract description 20
• 239000000612 proton pump inhibitor Substances 0.000 title claims abstract description 20
• 238000011282 treatment Methods 0.000 title claims abstract description 20
• 229940124003 CRTH2 antagonist Drugs 0.000 title abstract 3
• 150000003839 salts Chemical class 0.000 claims abstract description 137
• 229960004770 esomeprazole Drugs 0.000 claims abstract description 25
• SUBDBMMJDZJVOS-DEOSSOPVSA-N esomeprazole Chemical compound C([S@](=O)C1=NC2=CC=C(C=C2N1)OC)C1=NC=C(C)C(OC)=C1C SUBDBMMJDZJVOS-DEOSSOPVSA-N 0.000 claims abstract description 25
• SUBDBMMJDZJVOS-UHFFFAOYSA-N 5-methoxy-2-{[(4-methoxy-3,5-dimethylpyridin-2-yl)methyl]sulfinyl}-1H-benzimidazole Chemical compound N=1C2=CC(OC)=CC=C2NC=1S(=O)CC1=NC=C(C)C(OC)=C1C SUBDBMMJDZJVOS-UHFFFAOYSA-N 0.000 claims abstract description 22
• IQPSEEYGBUAQFF-UHFFFAOYSA-N Pantoprazole Chemical compound COC1=CC=NC(CS(=O)C=2NC3=CC=C(OC(F)F)C=C3N=2)=C1OC IQPSEEYGBUAQFF-UHFFFAOYSA-N 0.000 claims abstract description 22
• MJIHNNLFOKEZEW-UHFFFAOYSA-N lansoprazole Chemical compound CC1=C(OCC(F)(F)F)C=CN=C1CS(=O)C1=NC2=CC=CC=C2N1 MJIHNNLFOKEZEW-UHFFFAOYSA-N 0.000 claims abstract description 22
• 229960003174 lansoprazole Drugs 0.000 claims abstract description 22
• 229960000381 omeprazole Drugs 0.000 claims abstract description 22
• 229960005019 pantoprazole Drugs 0.000 claims abstract description 22
• 229960004157 rabeprazole Drugs 0.000 claims abstract description 22
• YREYEVIYCVEVJK-UHFFFAOYSA-N rabeprazole Chemical compound COCCCOC1=CC=NC(CS(=O)C=2NC3=CC=CC=C3N=2)=C1C YREYEVIYCVEVJK-UHFFFAOYSA-N 0.000 claims abstract description 22
• MJIHNNLFOKEZEW-RUZDIDTESA-N dexlansoprazole Chemical compound CC1=C(OCC(F)(F)F)C=CN=C1C[S@@](=O)C1=NC2=CC=CC=C2N1 MJIHNNLFOKEZEW-RUZDIDTESA-N 0.000 claims abstract description 21
• 229960003568 dexlansoprazole Drugs 0.000 claims abstract description 21
• 208000024891 symptom Diseases 0.000 claims abstract description 16
• 239000008194 pharmaceutical composition Substances 0.000 claims abstract 11
• QTBSBXVTEAMEQO-UHFFFAOYSA-N acetic acid Substances CC(O)=O QTBSBXVTEAMEQO-UHFFFAOYSA-N 0.000 claims description 587
• 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims description 122
• 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims description 113
• 125000000217 alkyl group Chemical group 0.000 claims description 103
• 239000005557 antagonist Substances 0.000 claims description 87
• 125000000593 indol-1-yl group Chemical group [H]C1=C([H])C([H])=C2N([*])C([H])=C([H])C2=C1[H] 0.000 claims description 82
• 125000000472 sulfonyl group Chemical group *S(*)(=O)=O 0.000 claims description 77
• 125000003118 aryl group Chemical group 0.000 claims description 62
• 125000001072 heteroaryl group Chemical group 0.000 claims description 49
• 150000001875 compounds Chemical class 0.000 claims description 46
• 229910052736 halogen Inorganic materials 0.000 claims description 46
• 229910052739 hydrogen Inorganic materials 0.000 claims description 43
• 239000001257 hydrogen Substances 0.000 claims description 38
• 125000001424 substituent group Chemical group 0.000 claims description 37
• 150000002367 halogens Chemical class 0.000 claims description 36
• 239000003246 corticosteroid Substances 0.000 claims description 32
• 125000000446 sulfanediyl group Chemical group *S* 0.000 claims description 27
• MVPPADPHJFYWMZ-UHFFFAOYSA-N chlorobenzene Substances ClC1=CC=CC=C1 MVPPADPHJFYWMZ-UHFFFAOYSA-N 0.000 claims description 18
• JUJWROOIHBZHMG-UHFFFAOYSA-N Pyridine Chemical compound C1=CC=NC=C1 JUJWROOIHBZHMG-UHFFFAOYSA-N 0.000 claims description 16
• FATGTHLOZSXOBC-UHFFFAOYSA-N 2-[5-fluoro-2-methyl-3-(quinolin-2-ylmethyl)indol-1-yl]acetic acid Chemical compound C12=CC(F)=CC=C2N(CC(O)=O)C(C)=C1CC1=CC=C(C=CC=C2)C2=N1 FATGTHLOZSXOBC-UHFFFAOYSA-N 0.000 claims description 14
• 125000000623 heterocyclic group Chemical group 0.000 claims description 13
• UFWIBTONFRDIAS-UHFFFAOYSA-N Naphthalene Chemical compound C1=CC=CC2=CC=CC=C21 UFWIBTONFRDIAS-UHFFFAOYSA-N 0.000 claims description 12
• SMWDFEZZVXVKRB-UHFFFAOYSA-N Quinoline Chemical compound N1=CC=CC2=CC=CC=C21 SMWDFEZZVXVKRB-UHFFFAOYSA-N 0.000 claims description 12
• YTPLMLYBLZKORZ-UHFFFAOYSA-N Thiophene Chemical compound C=1C=CSC=1 YTPLMLYBLZKORZ-UHFFFAOYSA-N 0.000 claims description 12
• 125000003349 3-pyridyl group Chemical group N1=C([H])C([*])=C([H])C([H])=C1[H] 0.000 claims description 11
• KAESVJOAVNADME-UHFFFAOYSA-N Pyrrole Chemical compound C=1C=CNC=1 KAESVJOAVNADME-UHFFFAOYSA-N 0.000 claims description 11
• 239000002253 acid Substances 0.000 claims description 11
• 229910052731 fluorine Inorganic materials 0.000 claims description 11
• 239000011737 fluorine Substances 0.000 claims description 11
• AWJUIBRHMBBTKR-UHFFFAOYSA-N isoquinoline Chemical compound C1=NC=CC2=CC=CC=C21 AWJUIBRHMBBTKR-UHFFFAOYSA-N 0.000 claims description 10
• VOVIALXJUBGFJZ-KWVAZRHASA-N Budesonide Chemical compound C1CC2=CC(=O)C=C[C@]2(C)[C@@H]2[C@@H]1[C@@H]1C[C@H]3OC(CCC)O[C@@]3(C(=O)CO)[C@@]1(C)C[C@@H]2O VOVIALXJUBGFJZ-KWVAZRHASA-N 0.000 claims description 8
• 229960004436 budesonide Drugs 0.000 claims description 8
• 125000002915 carbonyl group Chemical group [*:2]C([*:1])=O 0.000 claims description 8
• UMJSCPRVCHMLSP-UHFFFAOYSA-N pyridine Natural products COC1=CC=CN=C1 UMJSCPRVCHMLSP-UHFFFAOYSA-N 0.000 claims description 8
• XSCHRSMBECNVNS-UHFFFAOYSA-N quinoxaline Chemical compound N1=CC=NC2=CC=CC=C21 XSCHRSMBECNVNS-UHFFFAOYSA-N 0.000 claims description 8
• 239000012453 solvate Substances 0.000 claims description 8
• JYGXADMDTFJGBT-VWUMJDOOSA-N hydrocortisone Chemical compound O=C1CC[C@]2(C)[C@H]3[C@@H](O)C[C@](C)([C@@](CC4)(O)C(=O)CO)[C@@H]4[C@@H]3CCC2=C1 JYGXADMDTFJGBT-VWUMJDOOSA-N 0.000 claims description 6
• PYLWMHQQBFSUBP-UHFFFAOYSA-N monofluorobenzene Chemical compound FC1=CC=CC=C1 PYLWMHQQBFSUBP-UHFFFAOYSA-N 0.000 claims description 6
• 229930192474 thiophene Natural products 0.000 claims description 6
• 101100352202 Arabidopsis thaliana PIGA gene Proteins 0.000 claims description 5
• 229910052799 carbon Inorganic materials 0.000 claims description 5
• FZWLAAWBMGSTSO-UHFFFAOYSA-N Thiazole Chemical compound C1=CSC=N1 FZWLAAWBMGSTSO-UHFFFAOYSA-N 0.000 claims description 4
• 238000001574 biopsy Methods 0.000 claims description 4
• 238000011269 treatment regimen Methods 0.000 claims description 4
• AUHRDYPGCRKIKZ-UHFFFAOYSA-N 2-[2-methyl-3-(quinolin-2-ylmethyl)indol-1-yl]acetic acid Chemical compound C12=CC=CC=C2N(CC(O)=O)C(C)=C1CC1=CC=C(C=CC=C2)C2=N1 AUHRDYPGCRKIKZ-UHFFFAOYSA-N 0.000 claims description 3
• VHZQRDXTXVSINR-UHFFFAOYSA-N 2-[3-[(2-benzylsulfonylphenyl)methyl]-5-fluoro-2-methylindol-1-yl]acetic acid Chemical compound C12=CC(F)=CC=C2N(CC(O)=O)C(C)=C1CC1=CC=CC=C1S(=O)(=O)CC1=CC=CC=C1 VHZQRDXTXVSINR-UHFFFAOYSA-N 0.000 claims description 3
• BRNIUXLBABJPPA-UHFFFAOYSA-N 2-[3-[(4-benzylsulfonylphenyl)methyl]-5-fluoro-2-methylindol-1-yl]acetic acid Chemical compound C12=CC(F)=CC=C2N(CC(O)=O)C(C)=C1CC(C=C1)=CC=C1S(=O)(=O)CC1=CC=CC=C1 BRNIUXLBABJPPA-UHFFFAOYSA-N 0.000 claims description 3
• RCDLAJQERQUBRP-UHFFFAOYSA-N 2-[3-[[4-[(4-chlorophenyl)methylsulfonyl]phenyl]methyl]-5-fluoro-2-methylindol-1-yl]acetic acid Chemical compound C12=CC(F)=CC=C2N(CC(O)=O)C(C)=C1CC(C=C1)=CC=C1S(=O)(=O)CC1=CC=C(Cl)C=C1 RCDLAJQERQUBRP-UHFFFAOYSA-N 0.000 claims description 3
• QILUMBJCLHPTEK-UHFFFAOYSA-N 2-[5-chloro-2-methyl-3-(quinolin-2-ylmethyl)indol-1-yl]acetic acid Chemical compound C12=CC(Cl)=CC=C2N(CC(O)=O)C(C)=C1CC1=CC=C(C=CC=C2)C2=N1 QILUMBJCLHPTEK-UHFFFAOYSA-N 0.000 claims description 3
• PAKMLKICQKNIQV-UHFFFAOYSA-N 2-[5-fluoro-2-methyl-3-[(2-pyrrolidin-1-ylsulfonylphenyl)methyl]indol-1-yl]acetic acid Chemical compound C12=CC(F)=CC=C2N(CC(O)=O)C(C)=C1CC1=CC=CC=C1S(=O)(=O)N1CCCC1 PAKMLKICQKNIQV-UHFFFAOYSA-N 0.000 claims description 3
• UFWCTHMEWOEIES-UHFFFAOYSA-N 2-[5-fluoro-2-methyl-3-[(3-piperidin-1-ylsulfonylphenyl)methyl]indol-1-yl]acetic acid Chemical compound C12=CC(F)=CC=C2N(CC(O)=O)C(C)=C1CC(C=1)=CC=CC=1S(=O)(=O)N1CCCCC1 UFWCTHMEWOEIES-UHFFFAOYSA-N 0.000 claims description 3
• XUYPKIUZNJXPOQ-UHFFFAOYSA-N 2-[5-fluoro-2-methyl-3-[(3-pyrrolidin-1-ylsulfonylphenyl)methyl]indol-1-yl]acetic acid Chemical compound C12=CC(F)=CC=C2N(CC(O)=O)C(C)=C1CC(C=1)=CC=CC=1S(=O)(=O)N1CCCC1 XUYPKIUZNJXPOQ-UHFFFAOYSA-N 0.000 claims description 3
• ZENZJBGBJVAPCX-UHFFFAOYSA-N 2-[5-fluoro-2-methyl-3-[(4-piperidin-1-ylsulfonylphenyl)methyl]indol-1-yl]acetic acid Chemical compound C12=CC(F)=CC=C2N(CC(O)=O)C(C)=C1CC(C=C1)=CC=C1S(=O)(=O)N1CCCCC1 ZENZJBGBJVAPCX-UHFFFAOYSA-N 0.000 claims description 3
• WYZCOQATIZDSDW-UHFFFAOYSA-N 2-[5-fluoro-3-[[3-[(4-fluorophenyl)methylsulfonyl]phenyl]methyl]-2-methylindol-1-yl]acetic acid Chemical compound C12=CC(F)=CC=C2N(CC(O)=O)C(C)=C1CC(C=1)=CC=CC=1S(=O)(=O)CC1=CC=C(F)C=C1 WYZCOQATIZDSDW-UHFFFAOYSA-N 0.000 claims description 3
• NVXAOBKIOMYHKS-UHFFFAOYSA-N 2-[5-fluoro-3-[[4-[(4-fluorophenyl)methylsulfonyl]phenyl]methyl]-2-methylindol-1-yl]acetic acid Chemical compound C12=CC(F)=CC=C2N(CC(O)=O)C(C)=C1CC(C=C1)=CC=C1S(=O)(=O)CC1=CC=C(F)C=C1 NVXAOBKIOMYHKS-UHFFFAOYSA-N 0.000 claims description 3
• 125000000389 2-pyrrolyl group Chemical group [H]N1C([*])=C([H])C([H])=C1[H] 0.000 claims description 3
• FQISKWAFAHGMGT-SGJOWKDISA-M Methylprednisolone sodium succinate Chemical compound [Na+].C([C@@]12C)=CC(=O)C=C1[C@@H](C)C[C@@H]1[C@@H]2[C@@H](O)C[C@]2(C)[C@@](O)(C(=O)COC(=O)CCC([O-])=O)CC[C@H]21 FQISKWAFAHGMGT-SGJOWKDISA-M 0.000 claims description 3
• UCHDWCPVSPXUMX-TZIWLTJVSA-N Montelukast Chemical compound CC(C)(O)C1=CC=CC=C1CC[C@H](C=1C=C(\C=C\C=2N=C3C=C(Cl)C=CC3=CC=2)C=CC=1)SCC1(CC(O)=O)CC1 UCHDWCPVSPXUMX-TZIWLTJVSA-N 0.000 claims description 3
• 239000003795 chemical substances by application Substances 0.000 claims description 3
• 229960003957 dexamethasone Drugs 0.000 claims description 3
• UREBDLICKHMUKA-CXSFZGCWSA-N dexamethasone Chemical compound C1CC2=CC(=O)C=C[C@]2(C)[C@]2(F)[C@@H]1[C@@H]1C[C@@H](C)[C@@](C(=O)CO)(O)[C@@]1(C)C[C@@H]2O UREBDLICKHMUKA-CXSFZGCWSA-N 0.000 claims description 3
• 150000002148 esters Chemical class 0.000 claims description 3
• 229960002714 fluticasone Drugs 0.000 claims description 3
• MGNNYOODZCAHBA-GQKYHHCASA-N fluticasone Chemical compound C1([C@@H](F)C2)=CC(=O)C=C[C@]1(C)[C@]1(F)[C@@H]2[C@@H]2C[C@@H](C)[C@@](C(=O)SCF)(O)[C@@]2(C)C[C@@H]1O MGNNYOODZCAHBA-GQKYHHCASA-N 0.000 claims description 3
• 229960000890 hydrocortisone Drugs 0.000 claims description 3
• 125000002249 indol-2-yl group Chemical group [H]C1=C([H])C([H])=C2N([H])C([*])=C([H])C2=C1[H] 0.000 claims description 3
• 238000012423 maintenance Methods 0.000 claims description 3
• 229960004584 methylprednisolone Drugs 0.000 claims description 3
• 229960005127 montelukast Drugs 0.000 claims description 3
• 125000003396 thiol group Chemical group [H]S* 0.000 claims description 3
• NRPMXZUNAFYCRH-UHFFFAOYSA-N 2-[5-fluoro-2-methyl-3-[(2-piperidin-1-ylsulfonylphenyl)methyl]indol-1-yl]acetic acid Chemical compound C12=CC(F)=CC=C2N(CC(O)=O)C(C)=C1CC1=CC=CC=C1S(=O)(=O)N1CCCCC1 NRPMXZUNAFYCRH-UHFFFAOYSA-N 0.000 claims description 2
• 229960005205 prednisolone Drugs 0.000 claims description 2
• OIGNJSKKLXVSLS-VWUMJDOOSA-N prednisolone Chemical compound O=C1C=C[C@]2(C)[C@H]3[C@@H](O)C[C@](C)([C@@](CC4)(O)C(=O)CO)[C@@H]4[C@@H]3CCC2=C1 OIGNJSKKLXVSLS-VWUMJDOOSA-N 0.000 claims description 2
• UEMGWPRHOOEKTA-UHFFFAOYSA-N 1,3-difluorobenzene Chemical compound FC1=CC=CC(F)=C1 UEMGWPRHOOEKTA-UHFFFAOYSA-N 0.000 claims 1
• DJBHJFYUQAZFRB-UHFFFAOYSA-N 2-[3-[(2-cyclobutylsulfonylphenyl)methyl]-5-fluoro-2-methylindol-1-yl]acetic acid Chemical compound C12=CC(F)=CC=C2N(CC(O)=O)C(C)=C1CC1=CC=CC=C1S(=O)(=O)C1CCC1 DJBHJFYUQAZFRB-UHFFFAOYSA-N 0.000 claims 1
• WIOOBYGJMHMUPJ-UHFFFAOYSA-N 2-[3-[(2-cyclohexylsulfonylphenyl)methyl]-5-fluoro-2-methylindol-1-yl]acetic acid Chemical compound C12=CC(F)=CC=C2N(CC(O)=O)C(C)=C1CC1=CC=CC=C1S(=O)(=O)C1CCCCC1 WIOOBYGJMHMUPJ-UHFFFAOYSA-N 0.000 claims 1
• DSIZPFACZSRXAM-UHFFFAOYSA-N 2-[3-[(2-cyclopentylsulfonylphenyl)methyl]-5-fluoro-2-methylindol-1-yl]acetic acid Chemical compound C12=CC(F)=CC=C2N(CC(O)=O)C(C)=C1CC1=CC=CC=C1S(=O)(=O)C1CCCC1 DSIZPFACZSRXAM-UHFFFAOYSA-N 0.000 claims 1
• OJAHKYMVSLLQPG-UHFFFAOYSA-N 2-[3-[(3-benzylsulfonylphenyl)methyl]-5-fluoro-2-methylindol-1-yl]acetic acid Chemical compound C12=CC(F)=CC=C2N(CC(O)=O)C(C)=C1CC(C=1)=CC=CC=1S(=O)(=O)CC1=CC=CC=C1 OJAHKYMVSLLQPG-UHFFFAOYSA-N 0.000 claims 1
• GRCSJFWAKMMIDQ-UHFFFAOYSA-N 2-[3-[(4-cyclohexylsulfonylphenyl)methyl]-5-fluoro-2-methylindol-1-yl]acetic acid Chemical compound C12=CC(F)=CC=C2N(CC(O)=O)C(C)=C1CC(C=C1)=CC=C1S(=O)(=O)C1CCCCC1 GRCSJFWAKMMIDQ-UHFFFAOYSA-N 0.000 claims 1
• JZSPIXAOOJTSGW-UHFFFAOYSA-N 2-[3-[(4-cyclopentylsulfonylphenyl)methyl]-5-fluoro-2-methylindol-1-yl]acetic acid Chemical compound C12=CC(F)=CC=C2N(CC(O)=O)C(C)=C1CC(C=C1)=CC=C1S(=O)(=O)C1CCCC1 JZSPIXAOOJTSGW-UHFFFAOYSA-N 0.000 claims 1
• BFDRBVCOIAHTAN-UHFFFAOYSA-N 2-[5-fluoro-2-methyl-3-[(2-phenylphenyl)methyl]indol-1-yl]acetic acid Chemical compound C12=CC(F)=CC=C2N(CC(O)=O)C(C)=C1CC1=CC=CC=C1C1=CC=CC=C1 BFDRBVCOIAHTAN-UHFFFAOYSA-N 0.000 claims 1
• -1 dexlanoprazole Chemical compound 0.000 abstract description 94
• 230000009467 reduction Effects 0.000 abstract description 7
• 125000004531 indol-5-yl group Chemical group [H]N1C([H])=C([H])C2=C([H])C(*)=C([H])C([H])=C12 0.000 description 138
• 239000002552 dosage form Substances 0.000 description 49
• HYZJCKYKOHLVJF-UHFFFAOYSA-N 1H-benzimidazole Chemical compound C1=CC=C2NC=NC2=C1 HYZJCKYKOHLVJF-UHFFFAOYSA-N 0.000 description 46
• 125000006216 methylsulfinyl group Chemical group [H]C([H])([H])S(*)=O 0.000 description 43
• 125000002816 methylsulfanyl group Chemical group [H]C([H])([H])S[*] 0.000 description 36
• 125000005843 halogen group Chemical group 0.000 description 32
• 210000003979 eosinophil Anatomy 0.000 description 17
• 125000002924 primary amino group Chemical group [H]N([H])* 0.000 description 17
• 238000000034 method Methods 0.000 description 16
• 125000004435 hydrogen atom Chemical group [H]* 0.000 description 15
• HCUARRIEZVDMPT-UHFFFAOYSA-N Indole-2-carboxylic acid Chemical compound C1=CC=C2NC(C(=O)O)=CC2=C1 HCUARRIEZVDMPT-UHFFFAOYSA-N 0.000 description 14
• 150000002431 hydrogen Chemical class 0.000 description 14
• 239000000203 mixture Substances 0.000 description 14
• 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 description 13
• 210000003238 esophagus Anatomy 0.000 description 12
• 125000000951 phenoxy group Chemical group [H]C1=C([H])C([H])=C(O*)C([H])=C1[H] 0.000 description 12
• 229940068196 placebo Drugs 0.000 description 11
• 239000000902 placebo Substances 0.000 description 11
• 239000003826 tablet Substances 0.000 description 11
• SIKJAQJRHWYJAI-UHFFFAOYSA-N Indole Chemical compound C1=CC=C2NC=CC2=C1 SIKJAQJRHWYJAI-UHFFFAOYSA-N 0.000 description 9
• 239000011575 calcium Substances 0.000 description 9
• 125000000753 cycloalkyl group Chemical group 0.000 description 9
• 125000004169 (C1-C6) alkyl group Chemical group 0.000 description 8
• 206010048643 Hypereosinophilic syndrome Diseases 0.000 description 8
• 239000013543 active substance Substances 0.000 description 8
• 125000004429 atom Chemical group 0.000 description 8
• 125000001559 cyclopropyl group Chemical group [H]C1([H])C([H])([H])C1([H])* 0.000 description 8
• XBDQKXXYIPTUBI-UHFFFAOYSA-N dimethylselenoniopropionate Natural products CCC(O)=O XBDQKXXYIPTUBI-UHFFFAOYSA-N 0.000 description 8
• 208000021302 gastroesophageal reflux disease Diseases 0.000 description 8
• 210000003630 histaminocyte Anatomy 0.000 description 8
• 210000004027 cell Anatomy 0.000 description 7
• 210000005056 cell body Anatomy 0.000 description 7
• AQEFLFZSWDEAIP-UHFFFAOYSA-N di-tert-butyl ether Chemical compound CC(C)(C)OC(C)(C)C AQEFLFZSWDEAIP-UHFFFAOYSA-N 0.000 description 7
• 230000002327 eosinophilic effect Effects 0.000 description 7
• 239000007788 liquid Substances 0.000 description 7
• 125000004170 methylsulfonyl group Chemical group [H]C([H])([H])S(*)(=O)=O 0.000 description 7
• 125000003342 alkenyl group Chemical group 0.000 description 6
• 125000000304 alkynyl group Chemical group 0.000 description 6
• 125000004432 carbon atom Chemical group C* 0.000 description 6
• 230000000694 effects Effects 0.000 description 6
• 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 description 6
• 229910052757 nitrogen Inorganic materials 0.000 description 6
• 125000004433 nitrogen atom Chemical group N* 0.000 description 6
• PXGOKWXKJXAPGV-UHFFFAOYSA-N Fluorine Chemical compound FF PXGOKWXKJXAPGV-UHFFFAOYSA-N 0.000 description 5
• 206010030216 Oesophagitis Diseases 0.000 description 5
• 230000009471 action Effects 0.000 description 5
• 239000000460 chlorine Substances 0.000 description 5
• 229910052801 chlorine Inorganic materials 0.000 description 5
• 239000002702 enteric coating Substances 0.000 description 5
• 238000009505 enteric coating Methods 0.000 description 5
• 208000006881 esophagitis Diseases 0.000 description 5
• 239000008187 granular material Substances 0.000 description 5
• CZMRCDWAGMRECN-UGDNZRGBSA-N Sucrose Chemical compound O[C@H]1[C@H](O)[C@@H](CO)O[C@@]1(CO)O[C@@H]1[C@H](O)[C@@H](O)[C@H](O)[C@@H](CO)O1 CZMRCDWAGMRECN-UGDNZRGBSA-N 0.000 description 4
• 229930006000 Sucrose Natural products 0.000 description 4
• 238000009825 accumulation Methods 0.000 description 4
• 230000004913 activation Effects 0.000 description 4
• 125000002947 alkylene group Chemical group 0.000 description 4
• 239000013566 allergen Substances 0.000 description 4
• 230000015572 biosynthetic process Effects 0.000 description 4
• 239000000969 carrier Substances 0.000 description 4
• 229940079593 drug Drugs 0.000 description 4
• 239000003814 drug Substances 0.000 description 4
• 125000001153 fluoro group Chemical group F* 0.000 description 4
• 235000013305 food Nutrition 0.000 description 4
• 125000005842 heteroatom Chemical group 0.000 description 4
• RAXXELZNTBOGNW-UHFFFAOYSA-N imidazole Natural products C1=CNC=N1 RAXXELZNTBOGNW-UHFFFAOYSA-N 0.000 description 4
• PZOUSPYUWWUPPK-UHFFFAOYSA-N indole Natural products CC1=CC=CC2=C1C=CN2 PZOUSPYUWWUPPK-UHFFFAOYSA-N 0.000 description 4
• RKJUIXBNRJVNHR-UHFFFAOYSA-N indolenine Natural products C1=CC=C2CC=NC2=C1 RKJUIXBNRJVNHR-UHFFFAOYSA-N 0.000 description 4
• HQKMJHAJHXVSDF-UHFFFAOYSA-L magnesium stearate Chemical compound [Mg+2].CCCCCCCCCCCCCCCCCC([O-])=O.CCCCCCCCCCCCCCCCCC([O-])=O HQKMJHAJHXVSDF-UHFFFAOYSA-L 0.000 description 4
• 230000001404 mediated effect Effects 0.000 description 4
• 239000000651 prodrug Substances 0.000 description 4
• 229940002612 prodrug Drugs 0.000 description 4
• 150000003254 radicals Chemical class 0.000 description 4
• 230000004044 response Effects 0.000 description 4
• 239000011734 sodium Chemical class 0.000 description 4
• 229940083542 sodium Drugs 0.000 description 4
• 229910052708 sodium Inorganic materials 0.000 description 4
• 150000003431 steroids Chemical class 0.000 description 4
• 239000005720 sucrose Substances 0.000 description 4
• 229960004793 sucrose Drugs 0.000 description 4
• 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 description 4
• 125000004209 (C1-C8) alkyl group Chemical group 0.000 description 3
• HBAQYPYDRFILMT-UHFFFAOYSA-N 8-[3-(1-cyclopropylpyrazol-4-yl)-1H-pyrazolo[4,3-d]pyrimidin-5-yl]-3-methyl-3,8-diazabicyclo[3.2.1]octan-2-one Chemical class C1(CC1)N1N=CC(=C1)C1=NNC2=C1N=C(N=C2)N1C2C(N(CC1CC2)C)=O HBAQYPYDRFILMT-UHFFFAOYSA-N 0.000 description 3
• 102100037631 Centrin-2 Human genes 0.000 description 3
• 102000004127 Cytokines Human genes 0.000 description 3
• 108090000695 Cytokines Proteins 0.000 description 3
• 108010010803 Gelatin Proteins 0.000 description 3
• 101000880516 Homo sapiens Centrin-2 Proteins 0.000 description 3
• UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 description 3
• 206010061218 Inflammation Diseases 0.000 description 3
• 235000010643 Leucaena leucocephala Nutrition 0.000 description 3
• 240000007472 Leucaena leucocephala Species 0.000 description 3
• 125000003545 alkoxy group Chemical group 0.000 description 3
• 230000000172 allergic effect Effects 0.000 description 3
• 238000004458 analytical method Methods 0.000 description 3
• 208000010668 atopic eczema Diseases 0.000 description 3
• 239000011230 binding agent Substances 0.000 description 3
• 239000002775 capsule Substances 0.000 description 3
• 125000003917 carbamoyl group Chemical group [H]N([H])C(*)=O 0.000 description 3
• 230000008859 change Effects 0.000 description 3
• 125000001309 chloro group Chemical group Cl* 0.000 description 3
• 229960001334 corticosteroids Drugs 0.000 description 3
• 230000001419 dependent effect Effects 0.000 description 3
• 201000010099 disease Diseases 0.000 description 3
• 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 description 3
• 238000005516 engineering process Methods 0.000 description 3
• 229940014259 gelatin Drugs 0.000 description 3
• 239000008273 gelatin Substances 0.000 description 3
• 229920000159 gelatin Polymers 0.000 description 3
• 235000019322 gelatine Nutrition 0.000 description 3
• 235000011852 gelatine desserts Nutrition 0.000 description 3
• 230000004054 inflammatory process Effects 0.000 description 3
• VZCYOOQTPOCHFL-UPHRSURJSA-N maleic acid Chemical compound OC(=O)\C=C/C(O)=O VZCYOOQTPOCHFL-UPHRSURJSA-N 0.000 description 3
• 230000007170 pathology Effects 0.000 description 3
• 229950010765 pivalate Drugs 0.000 description 3
• IUGYQRQAERSCNH-UHFFFAOYSA-N pivalic acid Chemical compound CC(C)(C)C(O)=O IUGYQRQAERSCNH-UHFFFAOYSA-N 0.000 description 3
• 150000003460 sulfonic acids Chemical class 0.000 description 3
• 230000000699 topical effect Effects 0.000 description 3
• 125000006273 (C1-C3) alkyl group Chemical group 0.000 description 2
• 125000004178 (C1-C4) alkyl group Chemical group 0.000 description 2
• 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 description 2
• 125000006552 (C3-C8) cycloalkyl group Chemical group 0.000 description 2
• LBUJPTNKIBCYBY-UHFFFAOYSA-N 1,2,3,4-tetrahydroquinoline Chemical compound C1=CC=C2CCCNC2=C1 LBUJPTNKIBCYBY-UHFFFAOYSA-N 0.000 description 2
• VBICKXHEKHSIBG-UHFFFAOYSA-N 1-monostearoylglycerol Chemical compound CCCCCCCCCCCCCCCCCC(=O)OCC(O)CO VBICKXHEKHSIBG-UHFFFAOYSA-N 0.000 description 2
• BAXOFTOLAUCFNW-UHFFFAOYSA-N 1H-indazole Chemical compound C1=CC=C2C=NNC2=C1 BAXOFTOLAUCFNW-UHFFFAOYSA-N 0.000 description 2
• HZAXFHJVJLSVMW-UHFFFAOYSA-N 2-Aminoethan-1-ol Chemical compound NCCO HZAXFHJVJLSVMW-UHFFFAOYSA-N 0.000 description 2
• BYKXFHSGUBZCES-UHFFFAOYSA-N 2-[5-fluoro-2-methyl-3-(naphthalen-2-ylmethyl)indol-1-yl]acetic acid Chemical compound C12=CC(F)=CC=C2N(CC(O)=O)C(C)=C1CC1=CC=C(C=CC=C2)C2=C1 BYKXFHSGUBZCES-UHFFFAOYSA-N 0.000 description 2
• JRUNFSWRTCZPQT-UHFFFAOYSA-N 2-[5-fluoro-2-methyl-3-[(3-phenoxyphenyl)methyl]indol-1-yl]acetic acid Chemical compound C12=CC(F)=CC=C2N(CC(O)=O)C(C)=C1CC(C=1)=CC=CC=1OC1=CC=CC=C1 JRUNFSWRTCZPQT-UHFFFAOYSA-N 0.000 description 2
• VLTVKWWEZRRUFD-UHFFFAOYSA-N 2-[5-fluoro-2-methyl-3-[(3-phenoxythiophen-2-yl)methyl]indol-1-yl]acetic acid Chemical compound C12=CC(F)=CC=C2N(CC(O)=O)C(C)=C1CC=1SC=CC=1OC1=CC=CC=C1 VLTVKWWEZRRUFD-UHFFFAOYSA-N 0.000 description 2
• HJLPNIQIMSEBHY-UHFFFAOYSA-N 2-[5-fluoro-2-methyl-3-[(4-phenylphenyl)methyl]indol-1-yl]acetic acid Chemical compound C12=CC(F)=CC=C2N(CC(O)=O)C(C)=C1CC(C=C1)=CC=C1C1=CC=CC=C1 HJLPNIQIMSEBHY-UHFFFAOYSA-N 0.000 description 2
• QTBSBXVTEAMEQO-UHFFFAOYSA-M Acetate Chemical compound CC([O-])=O QTBSBXVTEAMEQO-UHFFFAOYSA-M 0.000 description 2
• GUBGYTABKSRVRQ-XLOQQCSPSA-N Alpha-Lactose Chemical compound O[C@@H]1[C@@H](O)[C@@H](O)[C@@H](CO)O[C@H]1O[C@@H]1[C@@H](CO)O[C@H](O)[C@H](O)[C@H]1O GUBGYTABKSRVRQ-XLOQQCSPSA-N 0.000 description 2
• 241000416162 Astragalus gummifer Species 0.000 description 2
• WKBOTKDWSSQWDR-UHFFFAOYSA-N Bromine atom Chemical compound [Br] WKBOTKDWSSQWDR-UHFFFAOYSA-N 0.000 description 2
• 206010008479 Chest Pain Diseases 0.000 description 2
• ZAMOUSCENKQFHK-UHFFFAOYSA-N Chlorine atom Chemical compound [Cl] ZAMOUSCENKQFHK-UHFFFAOYSA-N 0.000 description 2
• FBPFZTCFMRRESA-KVTDHHQDSA-N D-Mannitol Chemical compound OC[C@@H](O)[C@@H](O)[C@H](O)[C@H](O)CO FBPFZTCFMRRESA-KVTDHHQDSA-N 0.000 description 2
• 208000019505 Deglutition disease Diseases 0.000 description 2
• FEWJPZIEWOKRBE-JCYAYHJZSA-N Dextrotartaric acid Chemical compound OC(=O)[C@H](O)[C@@H](O)C(O)=O FEWJPZIEWOKRBE-JCYAYHJZSA-N 0.000 description 2
• 239000001856 Ethyl cellulose Substances 0.000 description 2
• ZZSNKZQZMQGXPY-UHFFFAOYSA-N Ethyl cellulose Chemical compound CCOCC1OC(OC)C(OCC)C(OCC)C1OC1C(O)C(O)C(OC)C(CO)O1 ZZSNKZQZMQGXPY-UHFFFAOYSA-N 0.000 description 2
• PEDCQBHIVMGVHV-UHFFFAOYSA-N Glycerine Chemical compound OCC(O)CO PEDCQBHIVMGVHV-UHFFFAOYSA-N 0.000 description 2
• 241000282414 Homo sapiens Species 0.000 description 2
• 206010020751 Hypersensitivity Diseases 0.000 description 2
• 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 2
• GUBGYTABKSRVRQ-QKKXKWKRSA-N Lactose Natural products OC[C@H]1O[C@@H](O[C@H]2[C@H](O)[C@@H](O)C(O)O[C@@H]2CO)[C@H](O)[C@@H](O)[C@H]1O GUBGYTABKSRVRQ-QKKXKWKRSA-N 0.000 description 2
• 229930195725 Mannitol Natural products 0.000 description 2
• 241001465754 Metazoa Species 0.000 description 2
• 208000030852 Parasitic disease Diseases 0.000 description 2
• FAPWRFPIFSIZLT-UHFFFAOYSA-M Sodium chloride Chemical compound [Na+].[Cl-] FAPWRFPIFSIZLT-UHFFFAOYSA-M 0.000 description 2
• 229920001615 Tragacanth Polymers 0.000 description 2
• 206010047700 Vomiting Diseases 0.000 description 2
• 125000002252 acyl group Chemical group 0.000 description 2
• 238000007259 addition reaction Methods 0.000 description 2
• 235000010443 alginic acid Nutrition 0.000 description 2
• 229920000615 alginic acid Polymers 0.000 description 2
• 150000001447 alkali salts Chemical class 0.000 description 2
• 208000026935 allergic disease Diseases 0.000 description 2
• 125000005605 benzo group Chemical group 0.000 description 2
• 229960002537 betamethasone Drugs 0.000 description 2
• UREBDLICKHMUKA-DVTGEIKXSA-N betamethasone Chemical compound C1CC2=CC(=O)C=C[C@]2(C)[C@]2(F)[C@@H]1[C@@H]1C[C@H](C)[C@@](C(=O)CO)(O)[C@@]1(C)C[C@@H]2O UREBDLICKHMUKA-DVTGEIKXSA-N 0.000 description 2
• GDTBXPJZTBHREO-UHFFFAOYSA-N bromine Substances BrBr GDTBXPJZTBHREO-UHFFFAOYSA-N 0.000 description 2
• 229910052794 bromium Inorganic materials 0.000 description 2
• CJZGTCYPCWQAJB-UHFFFAOYSA-L calcium stearate Chemical compound [Ca+2].CCCCCCCCCCCCCCCCCC([O-])=O.CCCCCCCCCCCCCCCCCC([O-])=O CJZGTCYPCWQAJB-UHFFFAOYSA-L 0.000 description 2
• 125000004093 cyano group Chemical group *C#N 0.000 description 2
• 125000004122 cyclic group Chemical group 0.000 description 2
• 239000003085 diluting agent Substances 0.000 description 2
• 238000001647 drug administration Methods 0.000 description 2
• 239000000839 emulsion Substances 0.000 description 2
• 235000019325 ethyl cellulose Nutrition 0.000 description 2
• 229920001249 ethyl cellulose Polymers 0.000 description 2
• 239000000796 flavoring agent Substances 0.000 description 2
• 235000013355 food flavoring agent Nutrition 0.000 description 2
• 150000004677 hydrates Chemical class 0.000 description 2
• 150000002460 imidazoles Chemical class 0.000 description 2
• WQJFIWXYPKYBTO-UHFFFAOYSA-N indole-1-acetic acid Chemical compound C1=CC=C2N(CC(=O)O)C=CC2=C1 WQJFIWXYPKYBTO-UHFFFAOYSA-N 0.000 description 2
• 239000000543 intermediate Substances 0.000 description 2
• 125000001449 isopropyl group Chemical group [H]C([H])([H])C([H])(*)C([H])([H])[H] 0.000 description 2
• 239000008101 lactose Substances 0.000 description 2
• 229960001375 lactose Drugs 0.000 description 2
• 239000007937 lozenge Substances 0.000 description 2
• 239000000314 lubricant Substances 0.000 description 2
• 235000019359 magnesium stearate Nutrition 0.000 description 2
• 235000010355 mannitol Nutrition 0.000 description 2
• 239000000594 mannitol Substances 0.000 description 2
• 229960001855 mannitol Drugs 0.000 description 2
• 238000004519 manufacturing process Methods 0.000 description 2
• 239000000463 material Substances 0.000 description 2
• 238000002483 medication Methods 0.000 description 2
• 229940126601 medicinal product Drugs 0.000 description 2
• 239000002207 metabolite Substances 0.000 description 2
• 229910052751 metal Inorganic materials 0.000 description 2
• 239000002184 metal Substances 0.000 description 2
• 150000002739 metals Chemical class 0.000 description 2
• 125000000956 methoxy group Chemical group [H]C([H])([H])O* 0.000 description 2
• VNXBKJFUJUWOCW-UHFFFAOYSA-N methylcyclopropane Chemical compound CC1CC1 VNXBKJFUJUWOCW-UHFFFAOYSA-N 0.000 description 2
• UHOVQNZJYSORNB-UHFFFAOYSA-N monobenzene Natural products C1=CC=CC=C1 UHOVQNZJYSORNB-UHFFFAOYSA-N 0.000 description 2
• 125000001624 naphthyl group Chemical group 0.000 description 2
• 239000003921 oil Substances 0.000 description 2
• 125000004043 oxo group Chemical group O=* 0.000 description 2
• 125000003854 p-chlorophenyl group Chemical group [H]C1=C([H])C(*)=C([H])C([H])=C1Cl 0.000 description 2
• 238000004806 packaging method and process Methods 0.000 description 2
• 125000003386 piperidinyl group Chemical group 0.000 description 2
• 229920000036 polyvinylpyrrolidone Polymers 0.000 description 2
• 235000013855 polyvinylpyrrolidone Nutrition 0.000 description 2
• 239000000843 powder Substances 0.000 description 2
• 229960002794 prednicarbate Drugs 0.000 description 2
• FNPXMHRZILFCKX-KAJVQRHHSA-N prednicarbate Chemical compound C1CC2=CC(=O)C=C[C@]2(C)[C@@H]2[C@@H]1[C@@H]1CC[C@@](C(=O)COC(=O)CC)(OC(=O)OCC)[C@@]1(C)C[C@@H]2O FNPXMHRZILFCKX-KAJVQRHHSA-N 0.000 description 2
• 229960004618 prednisone Drugs 0.000 description 2
• XOFYZVNMUHMLCC-ZPOLXVRWSA-N prednisone Chemical compound O=C1C=C[C@]2(C)[C@H]3C(=O)C[C@](C)([C@@](CC4)(O)C(=O)CO)[C@@H]4[C@@H]3CCC2=C1 XOFYZVNMUHMLCC-ZPOLXVRWSA-N 0.000 description 2
• 230000002265 prevention Effects 0.000 description 2
• 230000008569 process Effects 0.000 description 2
• 235000019260 propionic acid Nutrition 0.000 description 2
• 125000004076 pyridyl group Chemical group 0.000 description 2
• 125000000168 pyrrolyl group Chemical group 0.000 description 2
• 238000011160 research Methods 0.000 description 2
• 229930195734 saturated hydrocarbon Natural products 0.000 description 2
• 210000003491 skin Anatomy 0.000 description 2
• 210000002784 stomach Anatomy 0.000 description 2
• 230000002195 synergetic effect Effects 0.000 description 2
• 229940095064 tartrate Drugs 0.000 description 2
• 238000012360 testing method Methods 0.000 description 2
• 230000001225 therapeutic effect Effects 0.000 description 2
• 235000010487 tragacanth Nutrition 0.000 description 2
• 239000000196 tragacanth Substances 0.000 description 2
• 229940116362 tragacanth Drugs 0.000 description 2
• VZCYOOQTPOCHFL-UHFFFAOYSA-N trans-butenedioic acid Natural products OC(=O)C=CC(O)=O VZCYOOQTPOCHFL-UHFFFAOYSA-N 0.000 description 2
• XPDWGBQVDMORPB-UHFFFAOYSA-N trifluoromethane acid Natural products FC(F)F XPDWGBQVDMORPB-UHFFFAOYSA-N 0.000 description 2
• 230000008673 vomiting Effects 0.000 description 2
• 230000036642 wellbeing Effects 0.000 description 2
• LSPHULWDVZXLIL-UHFFFAOYSA-N (+/-)-Camphoric acid Chemical compound CC1(C)C(C(O)=O)CCC1(C)C(O)=O LSPHULWDVZXLIL-UHFFFAOYSA-N 0.000 description 1
• LNAZSHAWQACDHT-XIYTZBAFSA-N (2r,3r,4s,5r,6s)-4,5-dimethoxy-2-(methoxymethyl)-3-[(2s,3r,4s,5r,6r)-3,4,5-trimethoxy-6-(methoxymethyl)oxan-2-yl]oxy-6-[(2r,3r,4s,5r,6r)-4,5,6-trimethoxy-2-(methoxymethyl)oxan-3-yl]oxyoxane Chemical compound CO[C@@H]1[C@@H](OC)[C@H](OC)[C@@H](COC)O[C@H]1O[C@H]1[C@H](OC)[C@@H](OC)[C@H](O[C@H]2[C@@H]([C@@H](OC)[C@H](OC)O[C@@H]2COC)OC)O[C@@H]1COC LNAZSHAWQACDHT-XIYTZBAFSA-N 0.000 description 1
• 125000006527 (C1-C5) alkyl group Chemical group 0.000 description 1
• 125000004191 (C1-C6) alkoxy group Chemical group 0.000 description 1
• 125000006701 (C1-C7) alkyl group Chemical group 0.000 description 1
• GHOKWGTUZJEAQD-ZETCQYMHSA-N (D)-(+)-Pantothenic acid Chemical compound OCC(C)(C)[C@@H](O)C(=O)NCCC(O)=O GHOKWGTUZJEAQD-ZETCQYMHSA-N 0.000 description 1
• CSNIZNHTOVFARY-UHFFFAOYSA-N 1,2-benzothiazole Chemical compound C1=CC=C2C=NSC2=C1 CSNIZNHTOVFARY-UHFFFAOYSA-N 0.000 description 1
• FUOSTELFLYZQCW-UHFFFAOYSA-N 1,2-oxazol-3-one Chemical group OC=1C=CON=1 FUOSTELFLYZQCW-UHFFFAOYSA-N 0.000 description 1
• KBNBNXAWVBFVMI-UHFFFAOYSA-N 1-(1,1,2,2-tetrafluoroethoxy)benzimidazole Chemical compound C1=CC=C2N(OC(F)(F)C(F)F)C=NC2=C1 KBNBNXAWVBFVMI-UHFFFAOYSA-N 0.000 description 1
• LMGMINBSBGUQCT-UHFFFAOYSA-N 2-(2,5-dimethyl-3-quinolin-4-ylindol-1-yl)acetic acid Chemical compound C12=CC(C)=CC=C2N(CC(O)=O)C(C)=C1C1=CC=NC2=CC=CC=C12 LMGMINBSBGUQCT-UHFFFAOYSA-N 0.000 description 1
• ORRYGHOZQYKHGF-UHFFFAOYSA-N 2-(2-methyl-3-quinolin-4-ylindol-1-yl)acetic acid Chemical compound C12=CC=CC=C2N(CC(O)=O)C(C)=C1C1=CC=NC2=CC=CC=C12 ORRYGHOZQYKHGF-UHFFFAOYSA-N 0.000 description 1
• MOPTZNURXSTARI-UHFFFAOYSA-N 2-(5-chloro-2-methyl-3-quinolin-8-ylindol-1-yl)acetic acid Chemical compound C12=CC(Cl)=CC=C2N(CC(O)=O)C(C)=C1C1=CC=CC2=CC=CN=C12 MOPTZNURXSTARI-UHFFFAOYSA-N 0.000 description 1
• LJSREZMFZRABNJ-UHFFFAOYSA-N 2-[2,5-dimethyl-3-(7-methylquinolin-4-yl)indol-1-yl]acetic acid Chemical compound C12=CC(C)=CC=C2N(CC(O)=O)C(C)=C1C1=CC=NC2=CC(C)=CC=C12 LJSREZMFZRABNJ-UHFFFAOYSA-N 0.000 description 1
• PYCNZTVHCBCNPY-UHFFFAOYSA-N 2-[2,5-dimethyl-3-(8-methylquinolin-4-yl)indol-1-yl]acetic acid Chemical compound C12=CC(C)=CC=C2N(CC(O)=O)C(C)=C1C1=CC=NC2=C(C)C=CC=C12 PYCNZTVHCBCNPY-UHFFFAOYSA-N 0.000 description 1
• PVTFROQXBBAJHP-UHFFFAOYSA-N 2-[2,5-dimethyl-3-(8-nitroquinolin-4-yl)indol-1-yl]acetic acid Chemical compound C12=CC(C)=CC=C2N(CC(O)=O)C(C)=C1C1=CC=NC2=C([N+]([O-])=O)C=CC=C12 PVTFROQXBBAJHP-UHFFFAOYSA-N 0.000 description 1
• NHAKRBNTJVWOJY-UHFFFAOYSA-N 2-[2-methyl-3-(8-methylquinolin-4-yl)-5-(trifluoromethyl)indol-1-yl]acetic acid Chemical compound C12=CC(C(F)(F)F)=CC=C2N(CC(O)=O)C(C)=C1C1=CC=NC2=C(C)C=CC=C12 NHAKRBNTJVWOJY-UHFFFAOYSA-N 0.000 description 1
• RDXWQMSCRIJHDJ-UHFFFAOYSA-N 2-[3-(2,8-dimethylquinolin-4-yl)-2,5-dimethylindol-1-yl]acetic acid Chemical compound C12=CC(C)=CC=C2N(CC(O)=O)C(C)=C1C1=CC(C)=NC2=C(C)C=CC=C12 RDXWQMSCRIJHDJ-UHFFFAOYSA-N 0.000 description 1
• WTXWVKRBJGHPFW-UHFFFAOYSA-N 2-[3-(2-chloroquinolin-4-yl)-2,4-dimethylindol-1-yl]acetic acid Chemical compound C12=C(C)C=CC=C2N(CC(O)=O)C(C)=C1C1=CC(Cl)=NC2=CC=CC=C12 WTXWVKRBJGHPFW-UHFFFAOYSA-N 0.000 description 1
• GTAWSTRELDMZLI-UHFFFAOYSA-N 2-[3-(2-chloroquinolin-4-yl)-2,5-dimethylindol-1-yl]acetic acid Chemical compound C12=CC(C)=CC=C2N(CC(O)=O)C(C)=C1C1=CC(Cl)=NC2=CC=CC=C12 GTAWSTRELDMZLI-UHFFFAOYSA-N 0.000 description 1
• GEDIVZWJJNJULG-UHFFFAOYSA-N 2-[3-(2-chloroquinolin-4-yl)-2,6-dimethylindol-1-yl]acetic acid Chemical compound C12=CC=C(C)C=C2N(CC(O)=O)C(C)=C1C1=CC(Cl)=NC2=CC=CC=C12 GEDIVZWJJNJULG-UHFFFAOYSA-N 0.000 description 1
• GVNRQDCWXZDCRP-UHFFFAOYSA-N 2-[3-(2-chloroquinolin-4-yl)-2-methylindol-1-yl]acetic acid Chemical compound C12=CC=CC=C2N(CC(O)=O)C(C)=C1C1=CC(Cl)=NC2=CC=CC=C12 GVNRQDCWXZDCRP-UHFFFAOYSA-N 0.000 description 1
• WJGYTGOSWKIDGY-UHFFFAOYSA-N 2-[3-(2-chloroquinolin-4-yl)-5-methoxy-2-methylindol-1-yl]acetic acid Chemical compound C1=CC=C2C(C3=C(C)N(CC(O)=O)C4=CC=C(C=C43)OC)=CC(Cl)=NC2=C1 WJGYTGOSWKIDGY-UHFFFAOYSA-N 0.000 description 1
• SBTVBCDPBKMJAL-UHFFFAOYSA-N 2-[3-(2-chloroquinolin-4-yl)indol-1-yl]acetic acid Chemical compound C12=CC=CC=C2N(CC(=O)O)C=C1C1=CC(Cl)=NC2=CC=CC=C12 SBTVBCDPBKMJAL-UHFFFAOYSA-N 0.000 description 1
• SFUPNPSDGVIYIT-UHFFFAOYSA-N 2-[3-(4-chlorophenoxy)-2-methyl-4-pyrazin-2-ylindol-1-yl]acetic acid Chemical compound C12=C(C=3N=CC=NC=3)C=CC=C2N(CC(O)=O)C(C)=C1OC1=CC=C(Cl)C=C1 SFUPNPSDGVIYIT-UHFFFAOYSA-N 0.000 description 1
• JFDVCWFRJKHBAG-UHFFFAOYSA-N 2-[3-(4-chlorophenoxy)-2-methyl-5-methylsulfonylindol-1-yl]acetic acid Chemical compound C12=CC(S(C)(=O)=O)=CC=C2N(CC(O)=O)C(C)=C1OC1=CC=C(Cl)C=C1 JFDVCWFRJKHBAG-UHFFFAOYSA-N 0.000 description 1
• XFMGOBWEKPIIEZ-UHFFFAOYSA-N 2-[3-(4-cyanophenoxy)-2-methyl-5-(trifluoromethyl)indol-1-yl]acetic acid Chemical compound C12=CC(C(F)(F)F)=CC=C2N(CC(O)=O)C(C)=C1OC1=CC=C(C#N)C=C1 XFMGOBWEKPIIEZ-UHFFFAOYSA-N 0.000 description 1
• LPWWVNDAGZXRJB-UHFFFAOYSA-N 2-[3-(4-cyanophenoxy)-5-fluoro-2-methylindol-1-yl]acetic acid Chemical compound C12=CC(F)=CC=C2N(CC(O)=O)C(C)=C1OC1=CC=C(C#N)C=C1 LPWWVNDAGZXRJB-UHFFFAOYSA-N 0.000 description 1
• IOQWSIKRMSNYNH-UHFFFAOYSA-N 2-[3-(6,8-dimethylquinolin-4-yl)-2,5-dimethylindol-1-yl]acetic acid Chemical compound C12=CC(C)=CC=C2N(CC(O)=O)C(C)=C1C1=CC=NC2=C(C)C=C(C)C=C12 IOQWSIKRMSNYNH-UHFFFAOYSA-N 0.000 description 1
• FDHCUENRKQAIPG-UHFFFAOYSA-N 2-[3-(6-fluoroquinolin-4-yl)-2,5-dimethylindol-1-yl]acetic acid Chemical compound C12=CC(C)=CC=C2N(CC(O)=O)C(C)=C1C1=CC=NC2=CC=C(F)C=C12 FDHCUENRKQAIPG-UHFFFAOYSA-N 0.000 description 1
• LVUHPSMXFCXPEB-UHFFFAOYSA-N 2-[3-(6-methoxyquinolin-4-yl)-2,5-dimethylindol-1-yl]acetic acid Chemical compound C1=C(C)C=C2C(C3=CC=NC4=CC=C(C=C43)OC)=C(C)N(CC(O)=O)C2=C1 LVUHPSMXFCXPEB-UHFFFAOYSA-N 0.000 description 1
• DHWTVRVYTNGDGQ-UHFFFAOYSA-N 2-[3-(7-chloroquinolin-4-yl)-2,5-dimethyl-6-methylsulfonylindol-1-yl]acetic acid Chemical compound C12=CC(C)=C(S(C)(=O)=O)C=C2N(CC(O)=O)C(C)=C1C1=CC=NC2=CC(Cl)=CC=C12 DHWTVRVYTNGDGQ-UHFFFAOYSA-N 0.000 description 1
• KDRKEDVDJAVBAR-UHFFFAOYSA-N 2-[3-(7-chloroquinolin-4-yl)-2-methyl-5-methylsulfonylindol-1-yl]acetic acid Chemical compound C12=CC(S(C)(=O)=O)=CC=C2N(CC(O)=O)C(C)=C1C1=CC=NC2=CC(Cl)=CC=C12 KDRKEDVDJAVBAR-UHFFFAOYSA-N 0.000 description 1
• XBXOVKXPEXRXHT-UHFFFAOYSA-N 2-[3-(7-chloroquinolin-4-yl)-2-methyl-5-nitroindol-1-yl]acetic acid Chemical class C12=CC([N+]([O-])=O)=CC=C2N(CC(O)=O)C(C)=C1C1=CC=NC2=CC(Cl)=CC=C12 XBXOVKXPEXRXHT-UHFFFAOYSA-N 0.000 description 1
• ILHNFHPCCBAGBN-UHFFFAOYSA-N 2-[3-(7-chloroquinolin-4-yl)-4-methoxy-2-methylindol-1-yl]acetic acid Chemical compound ClC1=CC=C2C(C3=C(C)N(CC(O)=O)C=4C=CC=C(C3=4)OC)=CC=NC2=C1 ILHNFHPCCBAGBN-UHFFFAOYSA-N 0.000 description 1
• PZUBWDVPDYCNOI-UHFFFAOYSA-N 2-[3-(7-chloroquinolin-4-yl)-5-cyano-2-methylindol-1-yl]acetic acid Chemical compound C12=CC(C#N)=CC=C2N(CC(O)=O)C(C)=C1C1=CC=NC2=CC(Cl)=CC=C12 PZUBWDVPDYCNOI-UHFFFAOYSA-N 0.000 description 1
• HLIDFOBANPRHRY-UHFFFAOYSA-N 2-[3-(7-chloroquinolin-4-yl)-5-fluoro-2-methylindol-1-yl]acetic acid Chemical compound C12=CC(F)=CC=C2N(CC(O)=O)C(C)=C1C1=CC=NC2=CC(Cl)=CC=C12 HLIDFOBANPRHRY-UHFFFAOYSA-N 0.000 description 1
• NGISXSDIUBODBB-UHFFFAOYSA-N 2-[3-(8-bromo-2-methylquinolin-4-yl)-2,5-dimethylindol-1-yl]acetic acid Chemical compound C12=CC(C)=CC=C2N(CC(O)=O)C(C)=C1C1=CC(C)=NC2=C(Br)C=CC=C12 NGISXSDIUBODBB-UHFFFAOYSA-N 0.000 description 1
• GQXNIYGCBCQTRR-UHFFFAOYSA-N 2-[3-(8-chloroquinolin-4-yl)-2-methyl-5-methylsulfonylindol-1-yl]acetic acid Chemical compound C12=CC(S(C)(=O)=O)=CC=C2N(CC(O)=O)C(C)=C1C1=CC=NC2=C(Cl)C=CC=C12 GQXNIYGCBCQTRR-UHFFFAOYSA-N 0.000 description 1
• YSPMHWLGHPZYAS-UHFFFAOYSA-N 2-[3-(8-chloroquinolin-4-yl)-5-cyano-2-methylindol-1-yl]acetic acid Chemical compound C12=CC(C#N)=CC=C2N(CC(O)=O)C(C)=C1C1=CC=NC2=C(Cl)C=CC=C12 YSPMHWLGHPZYAS-UHFFFAOYSA-N 0.000 description 1
• VKWXZBKXISRUAL-UHFFFAOYSA-N 2-[3-(8-chloroquinolin-4-yl)-5-fluoro-2-methylindol-1-yl]acetic acid Chemical compound C12=CC(F)=CC=C2N(CC(O)=O)C(C)=C1C1=CC=NC2=C(Cl)C=CC=C12 VKWXZBKXISRUAL-UHFFFAOYSA-N 0.000 description 1
• XUGPSRPVEIUUDA-UHFFFAOYSA-N 2-[3-(8-cyanoquinolin-4-yl)-2,5-dimethylindol-1-yl]acetic acid Chemical compound C12=CC(C)=CC=C2N(CC(O)=O)C(C)=C1C1=CC=NC2=C(C#N)C=CC=C12 XUGPSRPVEIUUDA-UHFFFAOYSA-N 0.000 description 1
• XONPFUGOIKOYNU-UHFFFAOYSA-N 2-[3-(8-fluoroquinolin-4-yl)-2,5-dimethylindol-1-yl]acetic acid Chemical compound C12=CC(C)=CC=C2N(CC(O)=O)C(C)=C1C1=CC=NC2=C(F)C=CC=C12 XONPFUGOIKOYNU-UHFFFAOYSA-N 0.000 description 1
• XWRFXEGUGBWRKQ-UHFFFAOYSA-N 2-[3-(8-fluoroquinolin-4-yl)-2-methyl-5-(trifluoromethyl)indol-1-yl]acetic acid Chemical compound C12=CC(C(F)(F)F)=CC=C2N(CC(O)=O)C(C)=C1C1=CC=NC2=C(F)C=CC=C12 XWRFXEGUGBWRKQ-UHFFFAOYSA-N 0.000 description 1
• KGWGHTDRAPNYKZ-UHFFFAOYSA-N 2-[3-(8-methoxy-2-methylquinolin-4-yl)-2,5-dimethylindol-1-yl]acetic acid Chemical compound C1=C(C)C=C2C(C3=C4C=CC=C(C4=NC(C)=C3)OC)=C(C)N(CC(O)=O)C2=C1 KGWGHTDRAPNYKZ-UHFFFAOYSA-N 0.000 description 1
• SDHFXINHZHARIB-UHFFFAOYSA-N 2-[3-[2-(tert-butylsulfanylmethyl)-4-(2,2-dimethylpropanoylamino)phenoxy]-4-methoxyphenyl]acetic acid Chemical compound COC1=CC=C(CC(O)=O)C=C1OC1=CC=C(NC(=O)C(C)(C)C)C=C1CSC(C)(C)C SDHFXINHZHARIB-UHFFFAOYSA-N 0.000 description 1
• KVULPJIQOUYTAM-UHFFFAOYSA-N 2-[4-acetamido-3-(4-chlorophenoxy)-2-methylindol-1-yl]acetic acid Chemical compound C1=2C(NC(=O)C)=CC=CC=2N(CC(O)=O)C(C)=C1OC1=CC=C(Cl)C=C1 KVULPJIQOUYTAM-UHFFFAOYSA-N 0.000 description 1
• MGFCKFUBAHUJPN-UHFFFAOYSA-N 2-[5-acetamido-3-(7-chloroquinolin-4-yl)-2-methylindol-1-yl]acetic acid Chemical compound ClC1=CC=C2C(C3=C(C)N(CC(O)=O)C4=CC=C(C=C43)NC(=O)C)=CC=NC2=C1 MGFCKFUBAHUJPN-UHFFFAOYSA-N 0.000 description 1
• RGYQTNOUXRALCM-UHFFFAOYSA-N 2-[5-amino-3-(7-chloroquinolin-4-yl)-2-methylindol-1-yl]acetic acid Chemical compound C12=CC(N)=CC=C2N(CC(O)=O)C(C)=C1C1=CC=NC2=CC(Cl)=CC=C12 RGYQTNOUXRALCM-UHFFFAOYSA-N 0.000 description 1
• IZFCDILCIBKYGC-UHFFFAOYSA-N 2-[5-chloro-2-methyl-3-(8-methylquinolin-4-yl)indol-1-yl]acetic acid Chemical class C12=CC(Cl)=CC=C2N(CC(O)=O)C(C)=C1C1=CC=NC2=C(C)C=CC=C12 IZFCDILCIBKYGC-UHFFFAOYSA-N 0.000 description 1
• LCHNQSHWHSXOIB-UHFFFAOYSA-N 2-[5-chloro-3-(6-methoxy-2-methylquinolin-4-yl)-2-methylindol-1-yl]acetic acid Chemical class C1=C(Cl)C=C2C(C3=CC(C)=NC4=CC=C(C=C43)OC)=C(C)N(CC(O)=O)C2=C1 LCHNQSHWHSXOIB-UHFFFAOYSA-N 0.000 description 1
• WJAUASADFLGWGR-UHFFFAOYSA-N 2-[5-chloro-3-(7-chloroquinolin-4-yl)-2-(methoxymethyl)indol-1-yl]acetic acid Chemical compound C12=CC(Cl)=CC=C2N(CC(O)=O)C(COC)=C1C1=CC=NC2=CC(Cl)=CC=C12 WJAUASADFLGWGR-UHFFFAOYSA-N 0.000 description 1
• OJBCTDMMAARQHI-UHFFFAOYSA-N 2-[5-chloro-3-(7-chloroquinolin-4-yl)-2-methylindol-1-yl]acetic acid Chemical class C12=CC(Cl)=CC=C2N(CC(O)=O)C(C)=C1C1=CC=NC2=CC(Cl)=CC=C12 OJBCTDMMAARQHI-UHFFFAOYSA-N 0.000 description 1
• VBBYPIVGXYCSEO-UHFFFAOYSA-N 2-[5-cyano-2-methyl-3-(2-methylquinolin-4-yl)indol-1-yl]acetic acid Chemical compound C12=CC(C#N)=CC=C2N(CC(O)=O)C(C)=C1C1=CC(C)=NC2=CC=CC=C12 VBBYPIVGXYCSEO-UHFFFAOYSA-N 0.000 description 1
• FUUHQFJOTGHDLH-UHFFFAOYSA-N 2-[5-cyano-2-methyl-3-(8-methylquinolin-4-yl)indol-1-yl]acetic acid Chemical compound C12=CC(C#N)=CC=C2N(CC(O)=O)C(C)=C1C1=CC=NC2=C(C)C=CC=C12 FUUHQFJOTGHDLH-UHFFFAOYSA-N 0.000 description 1
• GSMAWHWKCCIPRZ-UHFFFAOYSA-N 2-[5-fluoro-2-methyl-3-(7-methylquinolin-4-yl)indol-1-yl]acetic acid Chemical compound C12=CC(F)=CC=C2N(CC(O)=O)C(C)=C1C1=CC=NC2=CC(C)=CC=C12 GSMAWHWKCCIPRZ-UHFFFAOYSA-N 0.000 description 1
• VUJRIDRKLRUVEH-UHFFFAOYSA-N 2-[5-fluoro-2-methyl-3-(8-methylquinolin-4-yl)indol-1-yl]acetic acid Chemical compound C12=CC(F)=CC=C2N(CC(O)=O)C(C)=C1C1=CC=NC2=C(C)C=CC=C12 VUJRIDRKLRUVEH-UHFFFAOYSA-N 0.000 description 1
• LNOOKYMYHBCVPL-UHFFFAOYSA-N 2-[5-methoxy-2-methyl-3-(8-methylquinolin-4-yl)indol-1-yl]acetic acid Chemical class C1=CC=C2C(C3=C(C)N(CC(O)=O)C4=CC=C(C=C43)OC)=CC=NC2=C1C LNOOKYMYHBCVPL-UHFFFAOYSA-N 0.000 description 1
• FTMFDXWHZNPHGR-UHFFFAOYSA-N 2-[[3-methyl-4-(2,2,2-trifluoroethoxy)pyridin-2-yl]methylsulfinyl]-6-(trifluoromethyl)-1h-benzimidazole Chemical compound CC1=C(OCC(F)(F)F)C=CN=C1CS(=O)C1=NC2=CC=C(C(F)(F)F)C=C2N1 FTMFDXWHZNPHGR-UHFFFAOYSA-N 0.000 description 1
• 125000000022 2-aminoethyl group Chemical group [H]C([*])([H])C([H])([H])N([H])[H] 0.000 description 1
• 125000001340 2-chloroethyl group Chemical group [H]C([H])(Cl)C([H])([H])* 0.000 description 1
• NEAQRZUHTPSBBM-UHFFFAOYSA-N 2-hydroxy-3,3-dimethyl-7-nitro-4h-isoquinolin-1-one Chemical group C1=C([N+]([O-])=O)C=C2C(=O)N(O)C(C)(C)CC2=C1 NEAQRZUHTPSBBM-UHFFFAOYSA-N 0.000 description 1
• JSKFHXHKTDLYTE-UHFFFAOYSA-N 2-indol-1-yl-2-methylpropanoic acid Chemical compound C1=CC=C2N(C(C)(C(O)=O)C)C=CC2=C1 JSKFHXHKTDLYTE-UHFFFAOYSA-N 0.000 description 1
• 229940080296 2-naphthalenesulfonate Drugs 0.000 description 1
• WPWNEKFMGCWNPR-UHFFFAOYSA-N 3,4-dihydro-2h-thiochromene Chemical compound C1=CC=C2CCCSC2=C1 WPWNEKFMGCWNPR-UHFFFAOYSA-N 0.000 description 1
• XMIIGOLPHOKFCH-UHFFFAOYSA-M 3-phenylpropionate Chemical compound [O-]C(=O)CCC1=CC=CC=C1 XMIIGOLPHOKFCH-UHFFFAOYSA-M 0.000 description 1
• JZRIZGDEYMWJKQ-UHFFFAOYSA-N 4-[1-(carboxymethyl)-5-chloro-2-methylindol-3-yl]oxybenzoic acid Chemical compound C12=CC(Cl)=CC=C2N(CC(O)=O)C(C)=C1OC1=CC=C(C(O)=O)C=C1 JZRIZGDEYMWJKQ-UHFFFAOYSA-N 0.000 description 1
• YVXQADDGUVCRDQ-UHFFFAOYSA-N 4-[1-(carboxymethyl)-5-fluoro-2-methylindol-3-yl]oxybenzoic acid Chemical compound C12=CC(F)=CC=C2N(CC(O)=O)C(C)=C1OC1=CC=C(C(O)=O)C=C1 YVXQADDGUVCRDQ-UHFFFAOYSA-N 0.000 description 1
• RJWBTWIBUIGANW-UHFFFAOYSA-N 4-chlorobenzenesulfonic acid Chemical compound OS(=O)(=O)C1=CC=C(Cl)C=C1 RJWBTWIBUIGANW-UHFFFAOYSA-N 0.000 description 1
• 125000004801 4-cyanophenyl group Chemical group [H]C1=C([H])C(C#N)=C([H])C([H])=C1* 0.000 description 1
• FHVDTGUDJYJELY-UHFFFAOYSA-N 6-{[2-carboxy-4,5-dihydroxy-6-(phosphanyloxy)oxan-3-yl]oxy}-4,5-dihydroxy-3-phosphanyloxane-2-carboxylic acid Chemical compound O1C(C(O)=O)C(P)C(O)C(O)C1OC1C(C(O)=O)OC(OP)C(O)C1O FHVDTGUDJYJELY-UHFFFAOYSA-N 0.000 description 1
• 125000001960 7 membered carbocyclic group Chemical group 0.000 description 1
• ZCYVEMRRCGMTRW-UHFFFAOYSA-N 7553-56-2 Chemical compound [I] ZCYVEMRRCGMTRW-UHFFFAOYSA-N 0.000 description 1
• 208000004998 Abdominal Pain Diseases 0.000 description 1
• 206010000087 Abdominal pain upper Diseases 0.000 description 1
• 241000282979 Alces alces Species 0.000 description 1
• 239000005995 Aluminium silicate Substances 0.000 description 1
• 241000271566 Aves Species 0.000 description 1
• 241000283690 Bos taurus Species 0.000 description 1
• 241000167854 Bourreria succulenta Species 0.000 description 1
• FERIUCNNQQJTOY-UHFFFAOYSA-M Butyrate Chemical compound CCCC([O-])=O FERIUCNNQQJTOY-UHFFFAOYSA-M 0.000 description 1
• FERIUCNNQQJTOY-UHFFFAOYSA-N Butyric acid Natural products CCCC(O)=O FERIUCNNQQJTOY-UHFFFAOYSA-N 0.000 description 1
• 125000000882 C2-C6 alkenyl group Chemical group 0.000 description 1
• 125000003601 C2-C6 alkynyl group Chemical group 0.000 description 1
• OYPRJOBELJOOCE-UHFFFAOYSA-N Calcium Chemical compound [Ca] OYPRJOBELJOOCE-UHFFFAOYSA-N 0.000 description 1
• 241000282472 Canis lupus familiaris Species 0.000 description 1
• 241000283707 Capra Species 0.000 description 1
• OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical group [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 description 1
• 102000005367 Carboxypeptidases Human genes 0.000 description 1
• 108010006303 Carboxypeptidases Proteins 0.000 description 1
• 229920000623 Cellulose acetate phthalate Polymers 0.000 description 1
• 241000282994 Cervidae Species 0.000 description 1
• KRKNYBCHXYNGOX-UHFFFAOYSA-K Citrate Chemical compound [O-]C(=O)CC(O)(CC([O-])=O)C([O-])=O KRKNYBCHXYNGOX-UHFFFAOYSA-K 0.000 description 1
• FBRAWBYQGRLCEK-AVVSTMBFSA-N Clobetasone butyrate Chemical compound C1CC2=CC(=O)C=C[C@]2(C)[C@]2(F)[C@@H]1[C@@H]1C[C@H](C)[C@@](C(=O)CCl)(OC(=O)CCC)[C@@]1(C)CC2=O FBRAWBYQGRLCEK-AVVSTMBFSA-N 0.000 description 1
• 208000035473 Communicable disease Diseases 0.000 description 1
• 229920002261 Corn starch Polymers 0.000 description 1
• ITRJWOMZKQRYTA-RFZYENFJSA-N Cortisone acetate Chemical compound C1CC2=CC(=O)CC[C@]2(C)[C@@H]2[C@@H]1[C@@H]1CC[C@@](C(=O)COC(=O)C)(O)[C@@]1(C)CC2=O ITRJWOMZKQRYTA-RFZYENFJSA-N 0.000 description 1
• 206010011224 Cough Diseases 0.000 description 1
• 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 description 1
• RGHNJXZEOKUKBD-SQOUGZDYSA-M D-gluconate Chemical compound OC[C@@H](O)[C@@H](O)[C@H](O)[C@@H](O)C([O-])=O RGHNJXZEOKUKBD-SQOUGZDYSA-M 0.000 description 1
• 235000019739 Dicalciumphosphate Nutrition 0.000 description 1
• 108010016626 Dipeptides Chemical group 0.000 description 1
• 241000283086 Equidae Species 0.000 description 1
• LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 description 1
• 241000282326 Felis catus Species 0.000 description 1
• WJOHZNCJWYWUJD-IUGZLZTKSA-N Fluocinonide Chemical compound C1([C@@H](F)C2)=CC(=O)C=C[C@]1(C)[C@]1(F)[C@@H]2[C@@H]2C[C@H]3OC(C)(C)O[C@@]3(C(=O)COC(=O)C)[C@@]2(C)C[C@@H]1O WJOHZNCJWYWUJD-IUGZLZTKSA-N 0.000 description 1
• WHZRCUIISKRTJL-YTZKRAOUSA-N Fluocortolone caproate Chemical compound C1([C@@H](F)C2)=CC(=O)C=C[C@]1(C)[C@@H]1[C@@H]2[C@@H]2C[C@@H](C)[C@H](C(=O)COC(=O)CCCCC)[C@@]2(C)C[C@@H]1O WHZRCUIISKRTJL-YTZKRAOUSA-N 0.000 description 1
• VZCYOOQTPOCHFL-OWOJBTEDSA-N Fumaric acid Chemical compound OC(=O)\C=C\C(O)=O VZCYOOQTPOCHFL-OWOJBTEDSA-N 0.000 description 1
• 241000282412 Homo Species 0.000 description 1
• VEXZGXHMUGYJMC-UHFFFAOYSA-N Hydrochloric acid Chemical class Cl VEXZGXHMUGYJMC-UHFFFAOYSA-N 0.000 description 1
• CPELXLSAUQHCOX-UHFFFAOYSA-N Hydrogen bromide Chemical class Br CPELXLSAUQHCOX-UHFFFAOYSA-N 0.000 description 1
• 102000003816 Interleukin-13 Human genes 0.000 description 1
• 108090000176 Interleukin-13 Proteins 0.000 description 1
• 102000004388 Interleukin-4 Human genes 0.000 description 1
• 108090000978 Interleukin-4 Proteins 0.000 description 1
• 102000000743 Interleukin-5 Human genes 0.000 description 1
• 108010002616 Interleukin-5 Proteins 0.000 description 1
• CKLJMWTZIZZHCS-REOHCLBHSA-N L-aspartic acid Chemical compound OC(=O)[C@@H](N)CC(O)=O CKLJMWTZIZZHCS-REOHCLBHSA-N 0.000 description 1
• JVTAAEKCZFNVCJ-UHFFFAOYSA-M Lactate Chemical compound CC(O)C([O-])=O JVTAAEKCZFNVCJ-UHFFFAOYSA-M 0.000 description 1
• FYYHWMGAXLPEAU-UHFFFAOYSA-N Magnesium Chemical compound [Mg] FYYHWMGAXLPEAU-UHFFFAOYSA-N 0.000 description 1
• 241000124008 Mammalia Species 0.000 description 1
• 241000343235 Maso Species 0.000 description 1
• 244000246386 Mentha pulegium Species 0.000 description 1
• 235000016257 Mentha pulegium Nutrition 0.000 description 1
• 235000004357 Mentha x piperita Nutrition 0.000 description 1
• AFVFQIVMOAPDHO-UHFFFAOYSA-N Methanesulfonic acid Chemical compound CS(O)(=O)=O AFVFQIVMOAPDHO-UHFFFAOYSA-N 0.000 description 1
• VVQNEPGJFQJSBK-UHFFFAOYSA-N Methyl methacrylate Chemical compound COC(=O)C(C)=C VVQNEPGJFQJSBK-UHFFFAOYSA-N 0.000 description 1
• 229920000168 Microcrystalline cellulose Polymers 0.000 description 1
• YNAVUWVOSKDBBP-UHFFFAOYSA-N Morpholine Chemical group C1COCCN1 YNAVUWVOSKDBBP-UHFFFAOYSA-N 0.000 description 1
• 241000699670 Mus sp. Species 0.000 description 1
• WHNWPMSKXPGLAX-UHFFFAOYSA-N N-Vinyl-2-pyrrolidone Chemical compound C=CN1CCCC1=O WHNWPMSKXPGLAX-UHFFFAOYSA-N 0.000 description 1
• 206010028813 Nausea Diseases 0.000 description 1
• PVNIIMVLHYAWGP-UHFFFAOYSA-N Niacin Chemical compound OC(=O)C1=CC=CN=C1 PVNIIMVLHYAWGP-UHFFFAOYSA-N 0.000 description 1
• MUBZPKHOEPUJKR-UHFFFAOYSA-N Oxalic acid Chemical compound OC(=O)C(O)=O MUBZPKHOEPUJKR-UHFFFAOYSA-N 0.000 description 1
• 208000002193 Pain Diseases 0.000 description 1
• 241001494479 Pecora Species 0.000 description 1
• 208000008469 Peptic Ulcer Diseases 0.000 description 1
• ZLMJMSJWJFRBEC-UHFFFAOYSA-N Potassium Chemical compound [K] ZLMJMSJWJFRBEC-UHFFFAOYSA-N 0.000 description 1
• CZPWVGJYEJSRLH-UHFFFAOYSA-N Pyrimidine Chemical group C1=CN=CN=C1 CZPWVGJYEJSRLH-UHFFFAOYSA-N 0.000 description 1
• 241000700159 Rattus Species 0.000 description 1
• 206010067171 Regurgitation Diseases 0.000 description 1
• NAQGHJTUZRHGAC-ZZZDFHIKSA-N SAICAR Chemical compound NC1=C(C(=O)N[C@@H](CC(O)=O)C(O)=O)N=CN1[C@H]1[C@H](O)[C@H](O)[C@@H](COP(O)(O)=O)O1 NAQGHJTUZRHGAC-ZZZDFHIKSA-N 0.000 description 1
• 244000180577 Sambucus australis Species 0.000 description 1
• 235000018734 Sambucus australis Nutrition 0.000 description 1
• 101100385396 Schizosaccharomyces pombe (strain 972 / ATCC 24843) cka1 gene Proteins 0.000 description 1
• VYPSYNLAJGMNEJ-UHFFFAOYSA-N Silicium dioxide Chemical compound O=[Si]=O VYPSYNLAJGMNEJ-UHFFFAOYSA-N 0.000 description 1
• 229920002472 Starch Polymers 0.000 description 1
• 235000021355 Stearic acid Nutrition 0.000 description 1
• 241000282887 Suidae Species 0.000 description 1
• QAOWNCQODCNURD-UHFFFAOYSA-L Sulfate Chemical class [O-]S([O-])(=O)=O QAOWNCQODCNURD-UHFFFAOYSA-L 0.000 description 1
• 210000001744 T-lymphocyte Anatomy 0.000 description 1
• ZMZDMBWJUHKJPS-UHFFFAOYSA-M Thiocyanate anion Chemical class [S-]C#N ZMZDMBWJUHKJPS-UHFFFAOYSA-M 0.000 description 1
• DTQVDTLACAAQTR-UHFFFAOYSA-M Trifluoroacetate Chemical compound [O-]C(=O)C(F)(F)F DTQVDTLACAAQTR-UHFFFAOYSA-M 0.000 description 1
• 102000001400 Tryptase Human genes 0.000 description 1
• 108060005989 Tryptase Proteins 0.000 description 1
• 206010047115 Vasculitis Diseases 0.000 description 1
• HCHKCACWOHOZIP-UHFFFAOYSA-N Zinc Chemical compound [Zn] HCHKCACWOHOZIP-UHFFFAOYSA-N 0.000 description 1
• 230000002159 abnormal effect Effects 0.000 description 1
• 125000000738 acetamido group Chemical group [H]C([H])([H])C(=O)N([H])[*] 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
• 239000004480 active ingredient Substances 0.000 description 1
• 239000000654 additive Substances 0.000 description 1
• 230000000996 additive effect Effects 0.000 description 1
• WNLRTRBMVRJNCN-UHFFFAOYSA-L adipate(2-) Chemical compound [O-]C(=O)CCCCC([O-])=O WNLRTRBMVRJNCN-UHFFFAOYSA-L 0.000 description 1
• 229940072056 alginate Drugs 0.000 description 1
• 239000000783 alginic acid Substances 0.000 description 1
• 229960001126 alginic acid Drugs 0.000 description 1
• 150000004781 alginic acids Chemical class 0.000 description 1
• 229910000287 alkaline earth metal oxide Inorganic materials 0.000 description 1
• 125000004453 alkoxycarbonyl group Chemical group 0.000 description 1
• 125000005079 alkoxycarbonylmethyl group Chemical group 0.000 description 1
• 125000005115 alkyl carbamoyl group Chemical group 0.000 description 1
• 125000005213 alkyl heteroaryl group Chemical group 0.000 description 1
• 125000004390 alkyl sulfonyl group Chemical group 0.000 description 1
• 208000030961 allergic reaction Diseases 0.000 description 1
• 230000007815 allergy Effects 0.000 description 1
• AWUCVROLDVIAJX-UHFFFAOYSA-N alpha-glycerophosphate Natural products OCC(O)COP(O)(O)=O AWUCVROLDVIAJX-UHFFFAOYSA-N 0.000 description 1
• 229910052782 aluminium Inorganic materials 0.000 description 1
• XAGFODPZIPBFFR-UHFFFAOYSA-N aluminium Chemical compound [Al] XAGFODPZIPBFFR-UHFFFAOYSA-N 0.000 description 1
• WNROFYMDJYEPJX-UHFFFAOYSA-K aluminium hydroxide Chemical compound [OH-].[OH-].[OH-].[Al+3] WNROFYMDJYEPJX-UHFFFAOYSA-K 0.000 description 1
• 235000012211 aluminium silicate Nutrition 0.000 description 1
• 229960003099 amcinonide Drugs 0.000 description 1
• ILKJAFIWWBXGDU-MOGDOJJUSA-N amcinonide Chemical compound O([C@@]1([C@H](O2)C[C@@H]3[C@@]1(C[C@H](O)[C@]1(F)[C@@]4(C)C=CC(=O)C=C4CC[C@H]13)C)C(=O)COC(=O)C)C12CCCC1 ILKJAFIWWBXGDU-MOGDOJJUSA-N 0.000 description 1
• 229940024606 amino acid Drugs 0.000 description 1
• 150000001413 amino acids Chemical group 0.000 description 1
• 238000010171 animal model Methods 0.000 description 1
• 239000000427 antigen Substances 0.000 description 1
• 102000036639 antigens Human genes 0.000 description 1
• 108091007433 antigens Proteins 0.000 description 1
• 230000006907 apoptotic process Effects 0.000 description 1
• 125000005116 aryl carbamoyl group Chemical group 0.000 description 1
• 125000005129 aryl carbonyl group Chemical group 0.000 description 1
• 125000001374 aryl-fused-cycloalkyl group Chemical group 0.000 description 1
• 125000000461 aryl-fused-heterocycloalkyl group Chemical group 0.000 description 1
• 229940009098 aspartate Drugs 0.000 description 1
• 230000002238 attenuated effect Effects 0.000 description 1
• 125000002393 azetidinyl group Chemical group 0.000 description 1
• 239000002585 base Substances 0.000 description 1
• 210000003651 basophil Anatomy 0.000 description 1
• RFRXIWQYSOIBDI-UHFFFAOYSA-N benzarone Chemical group CCC=1OC2=CC=CC=C2C=1C(=O)C1=CC=C(O)C=C1 RFRXIWQYSOIBDI-UHFFFAOYSA-N 0.000 description 1
• 229940077388 benzenesulfonate Drugs 0.000 description 1
• SRSXLGNVWSONIS-UHFFFAOYSA-M benzenesulfonate Chemical compound [O-]S(=O)(=O)C1=CC=CC=C1 SRSXLGNVWSONIS-UHFFFAOYSA-M 0.000 description 1
• 125000003785 benzimidazolyl group Chemical group N1=C(NC2=C1C=CC=C2)* 0.000 description 1
• 229940050390 benzoate Drugs 0.000 description 1
• WPYMKLBDIGXBTP-UHFFFAOYSA-N benzoic acid Chemical compound OC(=O)C1=CC=CC=C1 WPYMKLBDIGXBTP-UHFFFAOYSA-N 0.000 description 1
• 125000001797 benzyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])* 0.000 description 1
• 229910052790 beryllium Inorganic materials 0.000 description 1
• XMIIGOLPHOKFCH-UHFFFAOYSA-N beta-phenylpropanoic acid Natural products OC(=O)CCC1=CC=CC=C1 XMIIGOLPHOKFCH-UHFFFAOYSA-N 0.000 description 1
• 229960005354 betamethasone sodium phosphate Drugs 0.000 description 1
• PLCQGRYPOISRTQ-LWCNAHDDSA-L betamethasone sodium phosphate Chemical compound [Na+].[Na+].C1CC2=CC(=O)C=C[C@]2(C)[C@]2(F)[C@@H]1[C@@H]1C[C@H](C)[C@@](C(=O)COP([O-])([O-])=O)(O)[C@@]1(C)C[C@@H]2O PLCQGRYPOISRTQ-LWCNAHDDSA-L 0.000 description 1
• 229960004311 betamethasone valerate Drugs 0.000 description 1
• SNHRLVCMMWUAJD-SUYDQAKGSA-N betamethasone valerate Chemical compound C1CC2=CC(=O)C=C[C@]2(C)[C@]2(F)[C@@H]1[C@@H]1C[C@H](C)[C@@](C(=O)CO)(OC(=O)CCCC)[C@@]1(C)C[C@@H]2O SNHRLVCMMWUAJD-SUYDQAKGSA-N 0.000 description 1
• 239000000090 biomarker Substances 0.000 description 1
• 230000000903 blocking effect Effects 0.000 description 1
• 230000037396 body weight Effects 0.000 description 1
• 229950007227 buteprate Drugs 0.000 description 1
• 229910052791 calcium Inorganic materials 0.000 description 1
• 239000001506 calcium phosphate Substances 0.000 description 1
• 239000000378 calcium silicate Substances 0.000 description 1
• 229910052918 calcium silicate Inorganic materials 0.000 description 1
• 235000013539 calcium stearate Nutrition 0.000 description 1
• 239000008116 calcium stearate Substances 0.000 description 1
• OYACROKNLOSFPA-UHFFFAOYSA-N calcium;dioxido(oxo)silane Chemical compound [Ca+2].[O-][Si]([O-])=O OYACROKNLOSFPA-UHFFFAOYSA-N 0.000 description 1
• MIOPJNTWMNEORI-UHFFFAOYSA-N camphorsulfonic acid Chemical compound C1CC2(CS(O)(=O)=O)C(=O)CC1C2(C)C MIOPJNTWMNEORI-UHFFFAOYSA-N 0.000 description 1
• 150000001721 carbon Chemical group 0.000 description 1
• 239000001768 carboxy methyl cellulose Substances 0.000 description 1
• 125000004181 carboxyalkyl group Chemical group 0.000 description 1
• 150000001732 carboxylic acid derivatives Chemical group 0.000 description 1
• 150000001735 carboxylic acids Chemical class 0.000 description 1
• 229940081734 cellulose acetate phthalate Drugs 0.000 description 1
• 238000006243 chemical reaction Methods 0.000 description 1
• 230000003399 chemotactic effect Effects 0.000 description 1
• 235000019693 cherries Nutrition 0.000 description 1
• 239000007910 chewable tablet Substances 0.000 description 1
• QPAXMPYBNSHKAK-UHFFFAOYSA-N chloro(difluoro)methane Chemical group F[C](F)Cl QPAXMPYBNSHKAK-UHFFFAOYSA-N 0.000 description 1
• OEYIOHPDSNJKLS-UHFFFAOYSA-N choline Chemical compound C[N+](C)(C)CCO OEYIOHPDSNJKLS-UHFFFAOYSA-N 0.000 description 1
• 229960001231 choline Drugs 0.000 description 1
• 229940001468 citrate Drugs 0.000 description 1
• CBGUOGMQLZIXBE-XGQKBEPLSA-N clobetasol propionate Chemical compound C1CC2=CC(=O)C=C[C@]2(C)[C@]2(F)[C@@H]1[C@@H]1C[C@H](C)[C@@](C(=O)CCl)(OC(=O)CC)[C@@]1(C)C[C@@H]2O CBGUOGMQLZIXBE-XGQKBEPLSA-N 0.000 description 1
• 229960004703 clobetasol propionate Drugs 0.000 description 1
• 229960005465 clobetasone butyrate Drugs 0.000 description 1
• 238000011260 co-administration Methods 0.000 description 1
• 239000011248 coating agent Substances 0.000 description 1
• 238000000576 coating method Methods 0.000 description 1
• 229940075614 colloidal silicon dioxide Drugs 0.000 description 1
• 239000007891 compressed tablet Substances 0.000 description 1
• 230000006835 compression Effects 0.000 description 1
• 238000007906 compression Methods 0.000 description 1
• 238000013270 controlled release Methods 0.000 description 1
• 239000008120 corn starch Substances 0.000 description 1
• 229940099112 cornstarch Drugs 0.000 description 1
• BMCQMVFGOVHVNG-TUFAYURCSA-N cortisol 17-butyrate Chemical compound C1CC2=CC(=O)CC[C@]2(C)[C@@H]2[C@@H]1[C@@H]1CC[C@@](C(=O)CO)(OC(=O)CCC)[C@@]1(C)C[C@@H]2O BMCQMVFGOVHVNG-TUFAYURCSA-N 0.000 description 1
• FZCHYNWYXKICIO-FZNHGJLXSA-N cortisol 17-valerate Chemical compound C1CC2=CC(=O)CC[C@]2(C)[C@@H]2[C@@H]1[C@@H]1CC[C@@](C(=O)CO)(OC(=O)CCCC)[C@@]1(C)C[C@@H]2O FZCHYNWYXKICIO-FZNHGJLXSA-N 0.000 description 1
• ALEXXDVDDISNDU-JZYPGELDSA-N cortisol 21-acetate Chemical compound C1CC2=CC(=O)CC[C@]2(C)[C@@H]2[C@@H]1[C@@H]1CC[C@@](C(=O)COC(=O)C)(O)[C@@]1(C)C[C@@H]2O ALEXXDVDDISNDU-JZYPGELDSA-N 0.000 description 1
• 229960003290 cortisone acetate Drugs 0.000 description 1
• 125000006254 cycloalkyl carbonyl group Chemical group 0.000 description 1
• 125000001995 cyclobutyl group Chemical group [H]C1([H])C([H])([H])C([H])(*)C1([H])[H] 0.000 description 1
• 125000000113 cyclohexyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])(*)C([H])([H])C1([H])[H] 0.000 description 1
• JBDSSBMEKXHSJF-UHFFFAOYSA-N cyclopentanecarboxylic acid Chemical compound OC(=O)C1CCCC1 JBDSSBMEKXHSJF-UHFFFAOYSA-N 0.000 description 1
• 125000001511 cyclopentyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])(*)C1([H])[H] 0.000 description 1
• 230000003247 decreasing effect Effects 0.000 description 1
• 230000001934 delay Effects 0.000 description 1
• 229960003662 desonide Drugs 0.000 description 1
• WBGKWQHBNHJJPZ-LECWWXJVSA-N desonide Chemical compound C1CC2=CC(=O)C=C[C@]2(C)[C@@H]2[C@@H]1[C@@H]1C[C@H]3OC(C)(C)O[C@@]3(C(=O)CO)[C@@]1(C)C[C@@H]2O WBGKWQHBNHJJPZ-LECWWXJVSA-N 0.000 description 1
• 229960002344 dexamethasone sodium phosphate Drugs 0.000 description 1
• PLCQGRYPOISRTQ-FCJDYXGNSA-L dexamethasone sodium phosphate Chemical compound [Na+].[Na+].C1CC2=CC(=O)C=C[C@]2(C)[C@]2(F)[C@@H]1[C@@H]1C[C@@H](C)[C@@](C(=O)COP([O-])([O-])=O)(O)[C@@]1(C)C[C@@H]2O PLCQGRYPOISRTQ-FCJDYXGNSA-L 0.000 description 1
• 125000005117 dialkylcarbamoyl group Chemical group 0.000 description 1
• NEFBYIFKOOEVPA-UHFFFAOYSA-K dicalcium phosphate Chemical compound [Ca+2].[Ca+2].[O-]P([O-])([O-])=O NEFBYIFKOOEVPA-UHFFFAOYSA-K 0.000 description 1
• 229940038472 dicalcium phosphate Drugs 0.000 description 1
• 229910000390 dicalcium phosphate Inorganic materials 0.000 description 1
• OEBRKCOSUFCWJD-UHFFFAOYSA-N dichlorvos Chemical compound COP(=O)(OC)OC=C(Cl)Cl OEBRKCOSUFCWJD-UHFFFAOYSA-N 0.000 description 1
• ZBCBWPMODOFKDW-UHFFFAOYSA-N diethanolamine Chemical compound OCCNCCO ZBCBWPMODOFKDW-UHFFFAOYSA-N 0.000 description 1
• 239000002270 dispersing agent Substances 0.000 description 1
• 230000002183 duodenal effect Effects 0.000 description 1
• 239000000975 dye Substances 0.000 description 1
• 230000004064 dysfunction Effects 0.000 description 1
• 201000006549 dyspepsia Diseases 0.000 description 1
• 239000002662 enteric coated tablet Substances 0.000 description 1
• CCIVGXIOQKPBKL-UHFFFAOYSA-M ethanesulfonate Chemical compound CCS([O-])(=O)=O CCIVGXIOQKPBKL-UHFFFAOYSA-M 0.000 description 1
• 125000003754 ethoxycarbonyl group Chemical group C(=O)(OCC)* 0.000 description 1
• 230000007717 exclusion Effects 0.000 description 1
• 239000003889 eye drop Substances 0.000 description 1
• 229940012356 eye drops Drugs 0.000 description 1
• 239000000945 filler Substances 0.000 description 1
• 239000012530 fluid Substances 0.000 description 1
• 229960001347 fluocinolone acetonide Drugs 0.000 description 1
• FEBLZLNTKCEFIT-VSXGLTOVSA-N fluocinolone acetonide Chemical compound C1([C@@H](F)C2)=CC(=O)C=C[C@]1(C)[C@]1(F)[C@@H]2[C@@H]2C[C@H]3OC(C)(C)O[C@@]3(C(=O)CO)[C@@]2(C)C[C@@H]1O FEBLZLNTKCEFIT-VSXGLTOVSA-N 0.000 description 1
• 229960000785 fluocinonide Drugs 0.000 description 1
• 229960003973 fluocortolone Drugs 0.000 description 1
• GAKMQHDJQHZUTJ-ULHLPKEOSA-N fluocortolone Chemical compound C1([C@@H](F)C2)=CC(=O)C=C[C@]1(C)[C@@H]1[C@@H]2[C@@H]2C[C@@H](C)[C@H](C(=O)CO)[C@@]2(C)C[C@@H]1O GAKMQHDJQHZUTJ-ULHLPKEOSA-N 0.000 description 1
• 229960004437 fluocortolone caproate Drugs 0.000 description 1
• XZBJVIQXJHGUBE-HZMVJJPJSA-N fluocortolone pivalate Chemical compound C1([C@@H](F)C2)=CC(=O)C=C[C@]1(C)[C@@H]1[C@@H]2[C@@H]2C[C@@H](C)[C@H](C(=O)COC(=O)C(C)(C)C)[C@@]2(C)C[C@@H]1O XZBJVIQXJHGUBE-HZMVJJPJSA-N 0.000 description 1
• 229960005283 fluocortolone pivalate Drugs 0.000 description 1
• 125000002485 formyl group Chemical group [H]C(*)=O 0.000 description 1
• 239000007789 gas Substances 0.000 description 1
• 230000002496 gastric effect Effects 0.000 description 1
• 210000001035 gastrointestinal tract Anatomy 0.000 description 1
• 230000002068 genetic effect Effects 0.000 description 1
• 229940050410 gluconate Drugs 0.000 description 1
• 235000011187 glycerol Nutrition 0.000 description 1
• 125000004438 haloalkoxy group Chemical group 0.000 description 1
• 125000001188 haloalkyl group Chemical group 0.000 description 1
• 208000024798 heartburn Diseases 0.000 description 1
• MNWFXJYAOYHMED-UHFFFAOYSA-N heptanoic acid Chemical compound CCCCCCC(O)=O MNWFXJYAOYHMED-UHFFFAOYSA-N 0.000 description 1
• 125000000455 heteroaryl-fused-cycloalkyl group Chemical group 0.000 description 1
• 125000000643 heteroaryl-fused-heterocycloalkyl group Chemical group 0.000 description 1
• 125000005223 heteroarylcarbonyl group Chemical group 0.000 description 1
• FUZZWVXGSFPDMH-UHFFFAOYSA-N hexanoic acid Chemical compound CCCCCC(O)=O FUZZWVXGSFPDMH-UHFFFAOYSA-N 0.000 description 1
• 125000004051 hexyl group Chemical group [H]C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])* 0.000 description 1
• 235000012907 honey Nutrition 0.000 description 1
• 235000001050 hortel pimenta Nutrition 0.000 description 1
• 229960001067 hydrocortisone acetate Drugs 0.000 description 1
• 229960001524 hydrocortisone butyrate Drugs 0.000 description 1
• XMBWDFGMSWQBCA-UHFFFAOYSA-N hydrogen iodide Chemical class I XMBWDFGMSWQBCA-UHFFFAOYSA-N 0.000 description 1
• ZMZDMBWJUHKJPS-UHFFFAOYSA-N hydrogen thiocyanate Natural products SC#N ZMZDMBWJUHKJPS-UHFFFAOYSA-N 0.000 description 1
• QAOWNCQODCNURD-UHFFFAOYSA-M hydrogensulfate Chemical class OS([O-])(=O)=O QAOWNCQODCNURD-UHFFFAOYSA-M 0.000 description 1
• 125000002768 hydroxyalkyl group Chemical group 0.000 description 1
• 229920003063 hydroxymethyl cellulose Polymers 0.000 description 1
• 229940031574 hydroxymethyl cellulose Drugs 0.000 description 1
• 239000001866 hydroxypropyl methyl cellulose Substances 0.000 description 1
• 235000010979 hydroxypropyl methyl cellulose Nutrition 0.000 description 1
• 229920003088 hydroxypropyl methyl cellulose Polymers 0.000 description 1
• UFVKGYZPFZQRLF-UHFFFAOYSA-N hydroxypropyl methyl cellulose Chemical compound OC1C(O)C(OC)OC(CO)C1OC1C(O)C(O)C(OC2C(C(O)C(OC3C(C(O)C(O)C(CO)O3)O)C(CO)O2)O)C(CO)O1 UFVKGYZPFZQRLF-UHFFFAOYSA-N 0.000 description 1
• 125000002636 imidazolinyl group Chemical group 0.000 description 1
• 125000002883 imidazolyl group Chemical group 0.000 description 1
• 230000001900 immune effect Effects 0.000 description 1
• 239000003701 inert diluent Substances 0.000 description 1
• 208000015181 infectious disease Diseases 0.000 description 1
• 230000008595 infiltration Effects 0.000 description 1
• 238000001764 infiltration Methods 0.000 description 1
• 230000006749 inflammatory damage Effects 0.000 description 1
• 239000004615 ingredient Substances 0.000 description 1
• 238000002347 injection Methods 0.000 description 1
• 239000007924 injection Substances 0.000 description 1
• 230000003993 interaction Effects 0.000 description 1
• 229940028885 interleukin-4 Drugs 0.000 description 1
• 229940100602 interleukin-5 Drugs 0.000 description 1
• 238000007918 intramuscular administration Methods 0.000 description 1
• 238000001990 intravenous administration Methods 0.000 description 1
• 239000011630 iodine Substances 0.000 description 1
• 229910052740 iodine Inorganic materials 0.000 description 1
• SUMDYPCJJOFFON-UHFFFAOYSA-N isethionic acid Chemical compound OCCS(O)(=O)=O SUMDYPCJJOFFON-UHFFFAOYSA-N 0.000 description 1
• 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 1
• 229960000829 kaolin Drugs 0.000 description 1
• 229940001447 lactate Drugs 0.000 description 1
• 229940099584 lactobionate Drugs 0.000 description 1
• JYTUSYBCFIZPBE-AMTLMPIISA-N lactobionic acid Chemical compound OC(=O)[C@H](O)[C@@H](O)[C@@H]([C@H](O)CO)O[C@@H]1O[C@H](CO)[C@H](O)[C@H](O)[C@H]1O JYTUSYBCFIZPBE-AMTLMPIISA-N 0.000 description 1
• 206010024378 leukocytosis Diseases 0.000 description 1
• 210000004698 lymphocyte Anatomy 0.000 description 1
• 229910052749 magnesium Inorganic materials 0.000 description 1
• 239000011777 magnesium Substances 0.000 description 1
• ZLNQQNXFFQJAID-UHFFFAOYSA-L magnesium carbonate Chemical compound [Mg+2].[O-]C([O-])=O ZLNQQNXFFQJAID-UHFFFAOYSA-L 0.000 description 1
• 239000001095 magnesium carbonate Substances 0.000 description 1
• 229910000021 magnesium carbonate Inorganic materials 0.000 description 1
• VTHJTEIRLNZDEV-UHFFFAOYSA-L magnesium dihydroxide Chemical compound [OH-].[OH-].[Mg+2] VTHJTEIRLNZDEV-UHFFFAOYSA-L 0.000 description 1
• 239000000347 magnesium hydroxide Substances 0.000 description 1
• 229910001862 magnesium hydroxide Inorganic materials 0.000 description 1
• 239000000395 magnesium oxide Substances 0.000 description 1
• CPLXHLVBOLITMK-UHFFFAOYSA-N magnesium oxide Inorganic materials [Mg]=O CPLXHLVBOLITMK-UHFFFAOYSA-N 0.000 description 1
• AXZKOIWUVFPNLO-UHFFFAOYSA-N magnesium;oxygen(2-) Chemical compound [O-2].[Mg+2] AXZKOIWUVFPNLO-UHFFFAOYSA-N 0.000 description 1
• 230000014759 maintenance of location Effects 0.000 description 1
• 229940049920 malate Drugs 0.000 description 1
• BJEPYKJPYRNKOW-UHFFFAOYSA-N malic acid Chemical compound OC(=O)C(O)CC(O)=O BJEPYKJPYRNKOW-UHFFFAOYSA-N 0.000 description 1
• 230000007246 mechanism Effects 0.000 description 1
• 239000012907 medicinal substance Substances 0.000 description 1
• OGFXBIXJCWAUCH-UHFFFAOYSA-N meso-secoisolariciresinol Natural products C1=2C=C(O)C(OC)=CC=2CC(CO)C(CO)C1C1=CC=C(O)C(OC)=C1 OGFXBIXJCWAUCH-UHFFFAOYSA-N 0.000 description 1
• 229920003145 methacrylic acid copolymer Polymers 0.000 description 1
• 229920000609 methyl cellulose Polymers 0.000 description 1
• OSWPMRLSEDHDFF-UHFFFAOYSA-N methyl salicylate Chemical compound COC(=O)C1=CC=CC=C1O OSWPMRLSEDHDFF-UHFFFAOYSA-N 0.000 description 1
• 239000001923 methylcellulose Substances 0.000 description 1
• 235000010981 methylcellulose Nutrition 0.000 description 1
• 125000001570 methylene group Chemical group [H]C([H])([*:1])[*:2] 0.000 description 1
• 235000019813 microcrystalline cellulose Nutrition 0.000 description 1
• 239000008108 microcrystalline cellulose Substances 0.000 description 1
• 229940016286 microcrystalline cellulose Drugs 0.000 description 1
• 230000005012 migration Effects 0.000 description 1
• 238000013508 migration Methods 0.000 description 1
• 150000007522 mineralic acids Chemical class 0.000 description 1
• 239000007932 molded tablet Substances 0.000 description 1
• 229960001664 mometasone Drugs 0.000 description 1
• QLIIKPVHVRXHRI-CXSFZGCWSA-N mometasone Chemical compound C1CC2=CC(=O)C=C[C@]2(C)[C@]2(Cl)[C@@H]1[C@@H]1C[C@@H](C)[C@@](C(=O)CCl)(O)[C@@]1(C)C[C@@H]2O QLIIKPVHVRXHRI-CXSFZGCWSA-N 0.000 description 1
• 125000002757 morpholinyl group Chemical group 0.000 description 1
• 238000000465 moulding Methods 0.000 description 1
• 239000002324 mouth wash Substances 0.000 description 1
• 125000004108 n-butyl group Chemical group [H]C([H])([H])C([H])([H])C([H])([H])C([H])([H])* 0.000 description 1
• 125000001280 n-hexyl group Chemical group C(CCCCC)* 0.000 description 1
• 125000004123 n-propyl group Chemical group [H]C([H])([H])C([H])([H])C([H])([H])* 0.000 description 1
• KVBGVZZKJNLNJU-UHFFFAOYSA-M naphthalene-2-sulfonate Chemical compound C1=CC=CC2=CC(S(=O)(=O)[O-])=CC=C21 KVBGVZZKJNLNJU-UHFFFAOYSA-M 0.000 description 1
• 230000008693 nausea Effects 0.000 description 1
• 235000001968 nicotinic acid Nutrition 0.000 description 1
• 239000011664 nicotinic acid Substances 0.000 description 1
• 239000000820 nonprescription drug Substances 0.000 description 1
• QIQXTHQIDYTFRH-UHFFFAOYSA-N octadecanoic acid Chemical compound CCCCCCCCCCCCCCCCCC(O)=O QIQXTHQIDYTFRH-UHFFFAOYSA-N 0.000 description 1
• OQCDKBAXFALNLD-UHFFFAOYSA-N octadecanoic acid Natural products CCCCCCCC(C)CCCCCCCCC(O)=O OQCDKBAXFALNLD-UHFFFAOYSA-N 0.000 description 1
• 239000006186 oral dosage form Substances 0.000 description 1
• 229940100692 oral suspension Drugs 0.000 description 1
• 150000007524 organic acids Chemical class 0.000 description 1
• 235000005985 organic acids Nutrition 0.000 description 1
• 125000004430 oxygen atom Chemical group O* 0.000 description 1
• 229940014662 pantothenate Drugs 0.000 description 1
• 235000019161 pantothenic acid Nutrition 0.000 description 1
• 239000011713 pantothenic acid Substances 0.000 description 1
• 230000003076 paracrine Effects 0.000 description 1
• 239000002245 particle Substances 0.000 description 1
• 230000037361 pathway Effects 0.000 description 1
• 208000011906 peptic ulcer disease Diseases 0.000 description 1
• JRKICGRDRMAZLK-UHFFFAOYSA-L peroxydisulfate Chemical class [O-]S(=O)(=O)OOS([O-])(=O)=O JRKICGRDRMAZLK-UHFFFAOYSA-L 0.000 description 1
• 125000003356 phenylsulfanyl group Chemical group [*]SC1=C([H])C([H])=C([H])C([H])=C1[H] 0.000 description 1
• ACVYVLVWPXVTIT-UHFFFAOYSA-M phosphinate Chemical compound [O-][PH2]=O ACVYVLVWPXVTIT-UHFFFAOYSA-M 0.000 description 1
• 125000005541 phosphonamide group Chemical group 0.000 description 1
• UEZVMMHDMIWARA-UHFFFAOYSA-M phosphonate Chemical compound [O-]P(=O)=O UEZVMMHDMIWARA-UHFFFAOYSA-M 0.000 description 1
• 150000003016 phosphoric acids Chemical class 0.000 description 1
• 229910052698 phosphorus Inorganic materials 0.000 description 1
• XNGIFLGASWRNHJ-UHFFFAOYSA-L phthalate(2-) Chemical compound [O-]C(=O)C1=CC=CC=C1C([O-])=O XNGIFLGASWRNHJ-UHFFFAOYSA-L 0.000 description 1
• 229940075930 picrate Drugs 0.000 description 1
• OXNIZHLAWKMVMX-UHFFFAOYSA-M picrate anion Chemical compound [O-]C1=C([N+]([O-])=O)C=C([N+]([O-])=O)C=C1[N+]([O-])=O OXNIZHLAWKMVMX-UHFFFAOYSA-M 0.000 description 1
• 125000005936 piperidyl group Chemical group 0.000 description 1
• 229920001296 polysiloxane Polymers 0.000 description 1
• 229920002689 polyvinyl acetate Polymers 0.000 description 1
• 239000011118 polyvinyl acetate Substances 0.000 description 1
• 229940100467 polyvinyl acetate phthalate Drugs 0.000 description 1
• 239000001267 polyvinylpyrrolidone Substances 0.000 description 1
• 239000011591 potassium Substances 0.000 description 1
• 229910052700 potassium Inorganic materials 0.000 description 1
• 229940069328 povidone Drugs 0.000 description 1
• 239000003755 preservative agent Substances 0.000 description 1
• 230000002335 preservative effect Effects 0.000 description 1
• 238000003825 pressing Methods 0.000 description 1
• 125000001436 propyl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])[H] 0.000 description 1
• 150000003180 prostaglandins Chemical class 0.000 description 1
• 125000004528 pyrimidin-5-yl group Chemical group N1=CN=CC(=C1)* 0.000 description 1
• 125000000719 pyrrolidinyl group Chemical group 0.000 description 1
• 150000003248 quinolines Chemical class 0.000 description 1
• 125000005493 quinolyl group Chemical group 0.000 description 1
• 230000003979 response to food Effects 0.000 description 1
• 229910052702 rhenium Inorganic materials 0.000 description 1
• 229920006395 saturated elastomer Polymers 0.000 description 1
• 230000001932 seasonal effect Effects 0.000 description 1
• 239000010703 silicon Substances 0.000 description 1
• 229910052710 silicon Inorganic materials 0.000 description 1
• AWUCVROLDVIAJX-GSVOUGTGSA-N sn-glycerol 3-phosphate Chemical compound OC[C@@H](O)COP(O)(O)=O AWUCVROLDVIAJX-GSVOUGTGSA-N 0.000 description 1
• 235000019812 sodium carboxymethyl cellulose Nutrition 0.000 description 1
• 229920001027 sodium carboxymethylcellulose Polymers 0.000 description 1
• 239000011780 sodium chloride Substances 0.000 description 1
• 229960002668 sodium chloride Drugs 0.000 description 1
• 235000002639 sodium chloride Nutrition 0.000 description 1
• RYYKJJJTJZKILX-UHFFFAOYSA-M sodium octadecanoate Chemical compound [Na+].CCCCCCCCCCCCCCCCCC([O-])=O RYYKJJJTJZKILX-UHFFFAOYSA-M 0.000 description 1
• 239000007787 solid Substances 0.000 description 1
• 239000000243 solution Substances 0.000 description 1
• 239000000600 sorbitol Substances 0.000 description 1
• 229960002920 sorbitol Drugs 0.000 description 1
• 235000010356 sorbitol Nutrition 0.000 description 1
• 238000005507 spraying Methods 0.000 description 1
• 239000008107 starch Substances 0.000 description 1
• 229940032147 starch Drugs 0.000 description 1
• 235000019698 starch Nutrition 0.000 description 1
• 239000008117 stearic acid Substances 0.000 description 1
• 230000004936 stimulating effect Effects 0.000 description 1
• 230000000638 stimulation Effects 0.000 description 1
• 238000007920 subcutaneous administration Methods 0.000 description 1
• KDYFGRWQOYBRFD-UHFFFAOYSA-L succinate(2-) Chemical compound [O-]C(=O)CCC([O-])=O KDYFGRWQOYBRFD-UHFFFAOYSA-L 0.000 description 1
• 125000000475 sulfinyl group Chemical group [*:2]S([*:1])=O 0.000 description 1
• 239000004094 surface-active agent Substances 0.000 description 1
• 239000000725 suspension Substances 0.000 description 1
• 230000002459 sustained effect Effects 0.000 description 1
• 238000013268 sustained release Methods 0.000 description 1
• 230000009747 swallowing Effects 0.000 description 1
• 239000006188 syrup Substances 0.000 description 1
• 235000020357 syrup Nutrition 0.000 description 1
• 230000009885 systemic effect Effects 0.000 description 1
• 239000000454 talc Substances 0.000 description 1
• 229910052623 talc Inorganic materials 0.000 description 1
• 125000000999 tert-butyl group Chemical group [H]C([H])([H])C(*)(C([H])([H])[H])C([H])([H])[H] 0.000 description 1
• 125000005931 tert-butyloxycarbonyl group Chemical group [H]C([H])([H])C(OC(*)=O)(C([H])([H])[H])C([H])([H])[H] 0.000 description 1
• 125000003718 tetrahydrofuranyl group Chemical group 0.000 description 1
• 125000001412 tetrahydropyranyl group Chemical group 0.000 description 1
• NQRYJNQNLNOLGT-UHFFFAOYSA-N tetrahydropyridine hydrochloride Natural products C1CCNCC1 NQRYJNQNLNOLGT-UHFFFAOYSA-N 0.000 description 1
• 150000003536 tetrazoles Chemical group 0.000 description 1
• 125000002769 thiazolinyl group Chemical group 0.000 description 1
• 125000000335 thiazolyl group Chemical group 0.000 description 1
• 125000001544 thienyl group Chemical group 0.000 description 1
• 125000004568 thiomorpholinyl group Chemical group 0.000 description 1
• JOXIMZWYDAKGHI-UHFFFAOYSA-N toluene-4-sulfonic acid Chemical compound CC1=CC=C(S(O)(=O)=O)C=C1 JOXIMZWYDAKGHI-UHFFFAOYSA-N 0.000 description 1
• 229960005294 triamcinolone Drugs 0.000 description 1
• GFNANZIMVAIWHM-OBYCQNJPSA-N triamcinolone Chemical compound O=C1C=C[C@]2(C)[C@@]3(F)[C@@H](O)C[C@](C)([C@@]([C@H](O)C4)(O)C(=O)CO)[C@@H]4[C@@H]3CCC2=C1 GFNANZIMVAIWHM-OBYCQNJPSA-N 0.000 description 1
• 229960002117 triamcinolone acetonide Drugs 0.000 description 1
• YNDXUCZADRHECN-JNQJZLCISA-N triamcinolone acetonide Chemical compound C1CC2=CC(=O)C=C[C@]2(C)[C@]2(F)[C@@H]1[C@@H]1C[C@H]3OC(C)(C)O[C@@]3(C(=O)CO)[C@@]1(C)C[C@@H]2O YNDXUCZADRHECN-JNQJZLCISA-N 0.000 description 1
• ZDPHROOEEOARMN-UHFFFAOYSA-N undecanoic acid Chemical compound CCCCCCCCCCC(O)=O ZDPHROOEEOARMN-UHFFFAOYSA-N 0.000 description 1
• 239000011782 vitamin Substances 0.000 description 1
• 235000013343 vitamin Nutrition 0.000 description 1
• 229940088594 vitamin Drugs 0.000 description 1
• 229930003231 vitamin Natural products 0.000 description 1
• XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 description 1
• 239000009637 wintergreen oil Substances 0.000 description 1
• 229910052725 zinc Inorganic materials 0.000 description 1
• 239000011701 zinc Substances 0.000 description 1