RU2012110883A - Использование производных индола в качестве активаторов nurr-1 для их применения в качестве лекарственного средства для лечения болезни паркинсона - Google Patents
Использование производных индола в качестве активаторов nurr-1 для их применения в качестве лекарственного средства для лечения болезни паркинсона Download PDFInfo
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- RU2012110883A RU2012110883A RU2012110883/04A RU2012110883A RU2012110883A RU 2012110883 A RU2012110883 A RU 2012110883A RU 2012110883/04 A RU2012110883/04 A RU 2012110883/04A RU 2012110883 A RU2012110883 A RU 2012110883A RU 2012110883 A RU2012110883 A RU 2012110883A
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- Prior art keywords
- group
- methyl
- carbon atoms
- indol
- phenyl
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- 208000018737 Parkinson disease Diseases 0.000 title claims 4
- 239000012190 activator Substances 0.000 title 1
- 125000004432 carbon atom Chemical group C* 0.000 claims abstract 109
- 125000000217 alkyl group Chemical group 0.000 claims abstract 71
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims abstract 69
- 125000005843 halogen group Chemical group 0.000 claims abstract 46
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims abstract 33
- 125000003545 alkoxy group Chemical group 0.000 claims abstract 25
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims abstract 23
- 150000001875 compounds Chemical class 0.000 claims abstract 22
- 125000001072 heteroaryl group Chemical group 0.000 claims abstract 22
- 229910052799 carbon Inorganic materials 0.000 claims abstract 20
- 125000001424 substituent group Chemical group 0.000 claims abstract 19
- 125000003118 aryl group Chemical group 0.000 claims abstract 16
- 125000004122 cyclic group Chemical group 0.000 claims abstract 16
- 125000000623 heterocyclic group Chemical group 0.000 claims abstract 16
- 125000002915 carbonyl group Chemical group [*:2]C([*:1])=O 0.000 claims abstract 11
- 125000000951 phenoxy group Chemical group [H]C1=C([H])C([H])=C(O*)C([H])=C1[H] 0.000 claims abstract 11
- 125000004429 atom Chemical group 0.000 claims abstract 9
- 125000000816 ethylene group Chemical group [H]C([H])([*:1])C([H])([H])[*:2] 0.000 claims abstract 7
- 125000000753 cycloalkyl group Chemical group 0.000 claims abstract 5
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 claims abstract 5
- OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical compound [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 claims abstract 3
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 29
- 150000001721 carbon Chemical group 0.000 claims 14
- 125000001309 chloro group Chemical group Cl* 0.000 claims 12
- 229910052801 chlorine Inorganic materials 0.000 claims 8
- 229910052731 fluorine Inorganic materials 0.000 claims 8
- 125000001153 fluoro group Chemical group F* 0.000 claims 8
- QPJVMBTYPHYUOC-UHFFFAOYSA-N methyl benzoate Chemical compound COC(=O)C1=CC=CC=C1 QPJVMBTYPHYUOC-UHFFFAOYSA-N 0.000 claims 8
- 125000003226 pyrazolyl group Chemical group 0.000 claims 8
- 125000000472 sulfonyl group Chemical group *S(*)(=O)=O 0.000 claims 8
- 125000000999 tert-butyl group Chemical group [H]C([H])([H])C(*)(C([H])([H])[H])C([H])([H])[H] 0.000 claims 8
- 125000002843 carboxylic acid group Chemical group 0.000 claims 6
- 150000003839 salts Chemical class 0.000 claims 6
- 125000001544 thienyl group Chemical group 0.000 claims 6
- 230000002265 prevention Effects 0.000 claims 5
- ROSKYXAZUFLFLR-UHFFFAOYSA-N 4-[[1-(3-propan-2-ylphenyl)sulfonyl-5-(trifluoromethyl)indol-2-yl]methyl]benzoic acid Chemical compound CC(C)C1=CC=CC(S(=O)(=O)N2C3=CC=C(C=C3C=C2CC=2C=CC(=CC=2)C(O)=O)C(F)(F)F)=C1 ROSKYXAZUFLFLR-UHFFFAOYSA-N 0.000 claims 4
- -1 5 - [[1 - [(4-methyl-3,4-dihydro-2H-benzo [1,4] oxazin-6-yl) sulfonyl] -5-trifluoromethyl-1H-indol-2-yl] methyl] furan-3-carboxylic acid Chemical compound 0.000 claims 4
- VGGSQFUCUMXWEO-UHFFFAOYSA-N Ethene Chemical compound C=C VGGSQFUCUMXWEO-UHFFFAOYSA-N 0.000 claims 4
- 239000005977 Ethylene Substances 0.000 claims 4
- WPYMKLBDIGXBTP-UHFFFAOYSA-N benzoic acid Chemical compound OC(=O)C1=CC=CC=C1 WPYMKLBDIGXBTP-UHFFFAOYSA-N 0.000 claims 4
- 125000005433 dihydrobenzodioxinyl group Chemical group O1C(COC2=C1C=CC=C2)* 0.000 claims 4
- 125000005434 dihydrobenzoxazinyl group Chemical group O1N(CCC2=C1C=CC=C2)* 0.000 claims 4
- 125000002541 furyl group Chemical group 0.000 claims 4
- 125000000956 methoxy group Chemical group [H]C([H])([H])O* 0.000 claims 4
- 229910052757 nitrogen Inorganic materials 0.000 claims 4
- 125000004433 nitrogen atom Chemical group N* 0.000 claims 4
- 125000004076 pyridyl group Chemical group 0.000 claims 4
- 125000000168 pyrrolyl group Chemical group 0.000 claims 4
- 230000004770 neurodegeneration Effects 0.000 claims 3
- 208000015122 neurodegenerative disease Diseases 0.000 claims 3
- 239000008194 pharmaceutical composition Substances 0.000 claims 3
- FUOSTELFLYZQCW-UHFFFAOYSA-N 1,2-oxazol-3-one Chemical group OC=1C=CON=1 FUOSTELFLYZQCW-UHFFFAOYSA-N 0.000 claims 2
- FGYZXXJIDMOPDF-UHFFFAOYSA-N 2-fluoro-5-[[1-[(4-methyl-2,3-dihydro-1,4-benzoxazin-6-yl)sulfonyl]-5-(trifluoromethyl)indol-2-yl]methyl]benzoic acid Chemical compound C1=C2N(C)CCOC2=CC=C1S(=O)(=O)N(C1=CC=C(C=C1C=1)C(F)(F)F)C=1CC1=CC=C(F)C(C(O)=O)=C1 FGYZXXJIDMOPDF-UHFFFAOYSA-N 0.000 claims 2
- NWCDECRXMSNFFO-UHFFFAOYSA-N 3-[[1-(3-tert-butylphenyl)sulfonyl-5-(trifluoromethyl)indol-2-yl]methyl]-5-fluorobenzoic acid Chemical compound CC(C)(C)C1=CC=CC(S(=O)(=O)N2C3=CC=C(C=C3C=C2CC=2C=C(C=C(F)C=2)C(O)=O)C(F)(F)F)=C1 NWCDECRXMSNFFO-UHFFFAOYSA-N 0.000 claims 2
- RPKJDBOESOOANU-UHFFFAOYSA-N 4-[[1-(3-tert-butylphenyl)sulfonyl-3-fluoro-5-(trifluoromethyl)indol-2-yl]methyl]benzoic acid Chemical compound CC(C)(C)C1=CC=CC(S(=O)(=O)N2C3=CC=C(C=C3C(F)=C2CC=2C=CC(=CC=2)C(O)=O)C(F)(F)F)=C1 RPKJDBOESOOANU-UHFFFAOYSA-N 0.000 claims 2
- HXDYYHACDATIGB-UHFFFAOYSA-N 4-[[1-(3-tert-butylphenyl)sulfonyl-3-methyl-5-(trifluoromethyl)indol-2-yl]methyl]benzoic acid Chemical compound C=1C=CC(C(C)(C)C)=CC=1S(=O)(=O)N1C2=CC=C(C(F)(F)F)C=C2C(C)=C1CC1=CC=C(C(O)=O)C=C1 HXDYYHACDATIGB-UHFFFAOYSA-N 0.000 claims 2
- ODVJZYUUPXIGFU-UHFFFAOYSA-N 4-[[1-(3-tert-butylphenyl)sulfonyl-5-(trifluoromethyl)indol-2-yl]-fluoromethyl]benzoic acid Chemical compound CC(C)(C)C1=CC=CC(S(=O)(=O)N2C3=CC=C(C=C3C=C2C(F)C=2C=CC(=CC=2)C(O)=O)C(F)(F)F)=C1 ODVJZYUUPXIGFU-UHFFFAOYSA-N 0.000 claims 2
- WPEJKSVVMIDNBF-UHFFFAOYSA-N 4-[[1-(3-tert-butylphenyl)sulfonyl-5-(trifluoromethyl)indol-2-yl]-hydroxymethyl]-1-methylpyrrole-2-carboxylic acid Chemical compound C1=C(C(O)=O)N(C)C=C1C(O)C1=CC2=CC(C(F)(F)F)=CC=C2N1S(=O)(=O)C1=CC=CC(C(C)(C)C)=C1 WPEJKSVVMIDNBF-UHFFFAOYSA-N 0.000 claims 2
- SRKPQSVRGGJMSK-UHFFFAOYSA-N 4-[[1-(3-tert-butylphenyl)sulfonyl-5-(trifluoromethyl)indol-2-yl]methyl]-2-chlorobenzoic acid Chemical compound CC(C)(C)C1=CC=CC(S(=O)(=O)N2C3=CC=C(C=C3C=C2CC=2C=C(Cl)C(C(O)=O)=CC=2)C(F)(F)F)=C1 SRKPQSVRGGJMSK-UHFFFAOYSA-N 0.000 claims 2
- XLBPLVNGWMPZCX-UHFFFAOYSA-N 4-[[1-(3-tert-butylphenyl)sulfonyl-5-(trifluoromethyl)indol-2-yl]methyl]-3-fluorobenzoic acid Chemical compound CC(C)(C)C1=CC=CC(S(=O)(=O)N2C3=CC=C(C=C3C=C2CC=2C(=CC(=CC=2)C(O)=O)F)C(F)(F)F)=C1 XLBPLVNGWMPZCX-UHFFFAOYSA-N 0.000 claims 2
- CUIOROJHMZFUHV-UHFFFAOYSA-N 4-[[1-(3-tert-butylphenyl)sulfonyl-5-(trifluoromethyl)indol-2-yl]methyl]benzoic acid Chemical compound CC(C)(C)C1=CC=CC(S(=O)(=O)N2C3=CC=C(C=C3C=C2CC=2C=CC(=CC=2)C(O)=O)C(F)(F)F)=C1 CUIOROJHMZFUHV-UHFFFAOYSA-N 0.000 claims 2
- WDLWDEPSQUIFRH-UHFFFAOYSA-N 4-[[1-(3-tert-butylphenyl)sulfonyl-5-(trifluoromethyl)indol-2-yl]methyl]thiophene-2-carboxylic acid Chemical compound CC(C)(C)C1=CC=CC(S(=O)(=O)N2C3=CC=C(C=C3C=C2CC=2C=C(SC=2)C(O)=O)C(F)(F)F)=C1 WDLWDEPSQUIFRH-UHFFFAOYSA-N 0.000 claims 2
- OEUJREXTZMPFGO-UHFFFAOYSA-N 4-[[1-(4-propan-2-ylphenyl)sulfonyl-5-(trifluoromethyl)indol-2-yl]methyl]thiophene-2-carboxylic acid Chemical compound C1=CC(C(C)C)=CC=C1S(=O)(=O)N1C2=CC=C(C(F)(F)F)C=C2C=C1CC1=CSC(C(O)=O)=C1 OEUJREXTZMPFGO-UHFFFAOYSA-N 0.000 claims 2
- KPEJAILDLJYKHG-UHFFFAOYSA-N 4-[[1-[(4-methyl-2,3-dihydro-1,4-benzoxazin-6-yl)sulfonyl]-5-(trifluoromethyl)indol-2-yl]methyl]thiophene-2-carboxylic acid Chemical compound C1=C2N(C)CCOC2=CC=C1S(=O)(=O)N(C1=CC=C(C=C1C=1)C(F)(F)F)C=1CC1=CSC(C(O)=O)=C1 KPEJAILDLJYKHG-UHFFFAOYSA-N 0.000 claims 2
- KKOQRXIKLQBFFG-UHFFFAOYSA-N 4a,5-dihydro-4h-1,2-benzoxazin-3-one Chemical group C1C=CC=C2ONC(=O)CC21 KKOQRXIKLQBFFG-UHFFFAOYSA-N 0.000 claims 2
- XPPQVLKKEJEAPS-UHFFFAOYSA-N 5-[[1-(3-tert-butylphenyl)sulfonyl-5-(trifluoromethyl)indol-2-yl]methyl]-2-fluorobenzoic acid Chemical compound CC(C)(C)C1=CC=CC(S(=O)(=O)N2C3=CC=C(C=C3C=C2CC=2C=C(C(F)=CC=2)C(O)=O)C(F)(F)F)=C1 XPPQVLKKEJEAPS-UHFFFAOYSA-N 0.000 claims 2
- VXMWFBBAGIJGQA-UHFFFAOYSA-N 5-[[1-(3-tert-butylphenyl)sulfonyl-5-(trifluoromethyl)indol-2-yl]methyl]-2-methoxybenzoic acid Chemical compound C1=C(C(O)=O)C(OC)=CC=C1CC1=CC2=CC(C(F)(F)F)=CC=C2N1S(=O)(=O)C1=CC=CC(C(C)(C)C)=C1 VXMWFBBAGIJGQA-UHFFFAOYSA-N 0.000 claims 2
- BJKFUIAMKZHEPA-UHFFFAOYSA-N 5-[[1-(3-tert-butylphenyl)sulfonyl-5-(trifluoromethyl)indol-2-yl]methyl]-4-chloro-2-fluorobenzoic acid Chemical compound CC(C)(C)C1=CC=CC(S(=O)(=O)N2C3=CC=C(C=C3C=C2CC=2C(=CC(F)=C(C(O)=O)C=2)Cl)C(F)(F)F)=C1 BJKFUIAMKZHEPA-UHFFFAOYSA-N 0.000 claims 2
- TZGSLWYXBFXORX-UHFFFAOYSA-N 5-[[1-(3-tert-butylphenyl)sulfonyl-5-(trifluoromethyl)indol-2-yl]methyl]furan-2-carboxylic acid Chemical compound CC(C)(C)C1=CC=CC(S(=O)(=O)N2C3=CC=C(C=C3C=C2CC=2OC(=CC=2)C(O)=O)C(F)(F)F)=C1 TZGSLWYXBFXORX-UHFFFAOYSA-N 0.000 claims 2
- OJPWNWDQSVEPCD-UHFFFAOYSA-N 5-[[1-(3-tert-butylphenyl)sulfonyl-5-(trifluoromethyl)indol-2-yl]methyl]pyridine-3-carboxylic acid Chemical compound CC(C)(C)C1=CC=CC(S(=O)(=O)N2C3=CC=C(C=C3C=C2CC=2C=C(C=NC=2)C(O)=O)C(F)(F)F)=C1 OJPWNWDQSVEPCD-UHFFFAOYSA-N 0.000 claims 2
- UUAGKHRTIMLNQJ-UHFFFAOYSA-N 5-[[1-(4-propan-2-ylphenyl)sulfonyl-5-(trifluoromethyl)indol-2-yl]methyl]thiophene-2-carboxylic acid Chemical compound C1=CC(C(C)C)=CC=C1S(=O)(=O)N1C2=CC=C(C(F)(F)F)C=C2C=C1CC1=CC=C(C(O)=O)S1 UUAGKHRTIMLNQJ-UHFFFAOYSA-N 0.000 claims 2
- JKAFRUJWGWDYKJ-UHFFFAOYSA-N 5-[[1-[(4-methyl-2,3-dihydro-1,4-benzoxazin-6-yl)sulfonyl]-5-(trifluoromethyl)indol-2-yl]methyl]furan-2-carboxylic acid Chemical compound C1=C2N(C)CCOC2=CC=C1S(=O)(=O)N(C1=CC=C(C=C1C=1)C(F)(F)F)C=1CC1=CC=C(C(O)=O)O1 JKAFRUJWGWDYKJ-UHFFFAOYSA-N 0.000 claims 2
- RNDAEUVRHPPLGQ-UHFFFAOYSA-N 5-[[1-[(4-methyl-2,3-dihydro-1,4-benzoxazin-6-yl)sulfonyl]-5-(trifluoromethyl)indol-2-yl]methyl]thiophene-2-carboxylic acid Chemical compound C1=C2N(C)CCOC2=CC=C1S(=O)(=O)N(C1=CC=C(C=C1C=1)C(F)(F)F)C=1CC1=CC=C(C(O)=O)S1 RNDAEUVRHPPLGQ-UHFFFAOYSA-N 0.000 claims 2
- PSFFGWHJJQTRPR-UHFFFAOYSA-N 6-[[1-(3-tert-butylphenyl)sulfonyl-5-(trifluoromethyl)indol-2-yl]-hydroxymethyl]pyridine-3-carboxylic acid Chemical compound CC(C)(C)C1=CC=CC(S(=O)(=O)N2C3=CC=C(C=C3C=C2C(O)C=2N=CC(=CC=2)C(O)=O)C(F)(F)F)=C1 PSFFGWHJJQTRPR-UHFFFAOYSA-N 0.000 claims 2
- 239000005711 Benzoic acid Substances 0.000 claims 2
- WKBOTKDWSSQWDR-UHFFFAOYSA-N Bromine atom Chemical group [Br] WKBOTKDWSSQWDR-UHFFFAOYSA-N 0.000 claims 2
- 239000013543 active substance Substances 0.000 claims 2
- 125000000499 benzofuranyl group Chemical group O1C(=CC2=C1C=CC=C2)* 0.000 claims 2
- 235000010233 benzoic acid Nutrition 0.000 claims 2
- AQEFLFZSWDEAIP-UHFFFAOYSA-N di-tert-butyl ether Chemical compound CC(C)(C)OC(C)(C)C AQEFLFZSWDEAIP-UHFFFAOYSA-N 0.000 claims 2
- 125000000723 dihydrobenzofuranyl group Chemical group O1C(CC2=C1C=CC=C2)* 0.000 claims 2
- NVMYWDYCVSVNRR-UHFFFAOYSA-N ethyl 2-[[1-(3-tert-butylphenyl)sulfonyl-5-(trifluoromethyl)indol-2-yl]methyl]-1,3-thiazole-4-carboxylate Chemical compound CCOC(=O)C1=CSC(CC=2N(C3=CC=C(C=C3C=2)C(F)(F)F)S(=O)(=O)C=2C=C(C=CC=2)C(C)(C)C)=N1 NVMYWDYCVSVNRR-UHFFFAOYSA-N 0.000 claims 2
- 125000005842 heteroatom Chemical group 0.000 claims 2
- ATGVAQLUSGVYIV-UHFFFAOYSA-N methyl 4-[[1-(3-tert-butylphenyl)sulfonyl-3-fluoro-5-(trifluoromethyl)indol-2-yl]methyl]benzoate Chemical compound C1=CC(C(=O)OC)=CC=C1CC1=C(F)C2=CC(C(F)(F)F)=CC=C2N1S(=O)(=O)C1=CC=CC(C(C)(C)C)=C1 ATGVAQLUSGVYIV-UHFFFAOYSA-N 0.000 claims 2
- 125000002757 morpholinyl group Chemical group 0.000 claims 2
- HYDMZZSIDLERGE-UHFFFAOYSA-N n-[[4-[[1-(3-tert-butylphenyl)sulfonyl-5-(trifluoromethyl)indol-2-yl]methyl]phenyl]methyl]methanesulfonamide Chemical compound CC(C)(C)C1=CC=CC(S(=O)(=O)N2C3=CC=C(C=C3C=C2CC=2C=CC(CNS(C)(=O)=O)=CC=2)C(F)(F)F)=C1 HYDMZZSIDLERGE-UHFFFAOYSA-N 0.000 claims 2
- 125000001624 naphthyl group Chemical group 0.000 claims 2
- ZVTQYRVARPYRRE-UHFFFAOYSA-N oxadiazol-4-one Chemical group O=C1CON=N1 ZVTQYRVARPYRRE-UHFFFAOYSA-N 0.000 claims 2
- 125000003386 piperidinyl group Chemical group 0.000 claims 2
- 125000000719 pyrrolidinyl group Chemical group 0.000 claims 2
- 125000001712 tetrahydronaphthyl group Chemical group C1(CCCC2=CC=CC=C12)* 0.000 claims 2
- 125000000335 thiazolyl group Chemical group 0.000 claims 2
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 claims 2
- AILVULOTFQUVEJ-UHFFFAOYSA-N 4-[1-[1-(benzenesulfonyl)-5-methoxyindol-2-yl]-1-hydroxyethyl]pyridine-3-carboxylic acid Chemical compound C=1C2=CC(OC)=CC=C2N(S(=O)(=O)C=2C=CC=CC=2)C=1C(C)(O)C1=CC=NC=C1C(O)=O AILVULOTFQUVEJ-UHFFFAOYSA-N 0.000 claims 1
- XEPQMZRDLOFEAE-UHFFFAOYSA-N 4-[1-[1-(benzenesulfonyl)-5-methoxyindol-2-yl]ethyl]pyridine-3-carboxylic acid Chemical compound C=1C2=CC(OC)=CC=C2N(S(=O)(=O)C=2C=CC=CC=2)C=1C(C)C1=CC=NC=C1C(O)=O XEPQMZRDLOFEAE-UHFFFAOYSA-N 0.000 claims 1
- 239000003814 drug Substances 0.000 claims 1
- 238000004519 manufacturing process Methods 0.000 claims 1
- 125000002816 methylsulfanyl group Chemical group [H]C([H])([H])S[*] 0.000 claims 1
- 239000000546 pharmaceutical excipient Substances 0.000 claims 1
- 125000003170 phenylsulfonyl group Chemical group C1(=CC=CC=C1)S(=O)(=O)* 0.000 claims 1
- 239000002253 acid Substances 0.000 abstract 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D209/00—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
- C07D209/02—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
- C07D209/04—Indoles; Hydrogenated indoles
- C07D209/10—Indoles; Hydrogenated indoles with substituted hydrocarbon radicals attached to carbon atoms of the hetero ring
- C07D209/18—Radicals substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
- C07D209/26—Radicals substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals with an acyl radical attached to the ring nitrogen atom
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D209/00—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
- C07D209/02—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
- C07D209/04—Indoles; Hydrogenated indoles
- C07D209/10—Indoles; Hydrogenated indoles with substituted hydrocarbon radicals attached to carbon atoms of the hetero ring
-
- 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
- A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
- A61K31/403—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with carbocyclic rings, e.g. carbazole
- A61K31/404—Indoles, e.g. pindolol
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
- A61P25/16—Anti-Parkinson drugs
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D209/00—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
- C07D209/02—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
- C07D209/04—Indoles; Hydrogenated indoles
- C07D209/30—Indoles; Hydrogenated indoles with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to carbon atoms of the hetero ring
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
- C07D401/06—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
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- C07D405/12—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
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- C07D407/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen atoms as the only ring hetero atoms, not provided for by group C07D405/00 containing two hetero rings
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- C07D409/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
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- C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
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- C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
- C07D413/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
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- C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
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- C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
- C07D417/06—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
- C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
- C07D417/10—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a carbon chain containing aromatic rings
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- Chemical & Material Sciences (AREA)
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- Health & Medical Sciences (AREA)
- Engineering & Computer Science (AREA)
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- Biomedical Technology (AREA)
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- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
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Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| FR0956259A FR2950053B1 (fr) | 2009-09-11 | 2009-09-11 | Utilisation de derives d'indole benzoique comme activateurs de nurr-1, pour le traitement de la maladie de parkinson |
| FR0956259 | 2009-09-11 | ||
| FR1050107A FR2950058B1 (fr) | 2009-09-11 | 2010-01-08 | Utilisation de derives d'indole benzoique comme activateurs de nurr-1, pour le traitement de la maladie de parkinson |
| FR1050107 | 2010-01-08 | ||
| PCT/FR2010/051884 WO2011030068A1 (fr) | 2009-09-11 | 2010-09-10 | Utilisation de derives d'indole comme activateurs de nurr-1, pour leur application en tant que medicament pour le traitement de la maladie de parkinson |
Publications (1)
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| RU2012110883A true RU2012110883A (ru) | 2013-10-20 |
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| RU2012110883/04A RU2012110883A (ru) | 2009-09-11 | 2010-09-10 | Использование производных индола в качестве активаторов nurr-1 для их применения в качестве лекарственного средства для лечения болезни паркинсона |
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| CN105272975B (zh) * | 2014-06-10 | 2019-03-26 | 中国科学院上海药物研究所 | 一类具有1,2,4-恶二唑片段结构的吲哚生物碱及其制备方法和用途 |
| WO2018136575A1 (en) * | 2017-01-18 | 2018-07-26 | Albert Einstein College Of Medicine, Inc. | Pxr agonists and uses thereof for gut barrier dysfunction treatment and prevention |
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| ATE482945T1 (de) * | 1998-05-26 | 2010-10-15 | Chugai Pharmaceutical Co Ltd | Heterozyklische indolderivate und mono- oder diazaindol-derivate |
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| IL152477A0 (en) * | 2000-04-28 | 2003-05-29 | Baxter Healthcare Sa | 2-acyl indol derivatives and their use as anti-tumour agents |
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| DK1761519T3 (da) * | 2004-06-21 | 2008-07-21 | Hoffmann La Roche | Indolderivater som histaminreceptorantagonister |
| FR2890071B1 (fr) * | 2005-08-30 | 2007-11-09 | Fournier Sa Sa Lab | Nouveaux composes de l'indole |
| SG165362A1 (en) * | 2005-09-07 | 2010-10-28 | Plexxikon Inc | Ppar active compounds |
| FR2903107B1 (fr) | 2006-07-03 | 2008-08-22 | Sanofi Aventis Sa | Derives d'imidazopyridine-2-carboxamides, leur preparation et leur application en therapeutique |
| FR2903106B1 (fr) | 2006-07-03 | 2010-07-30 | Sanofi Aventis | Utilisations de 2-benzoyl-imidazopyridines en therapeutique |
| FR2903105A1 (fr) | 2006-07-03 | 2008-01-04 | Sanofi Aventis Sa | Derives de 2-benzoyl-imidazopyridines, leur preparation et leur application en therapeutique |
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2010
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Also Published As
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| IL218526A0 (en) | 2012-07-31 |
| MX2012003027A (es) | 2012-04-19 |
| US20120232070A1 (en) | 2012-09-13 |
| IN2012DN02005A (enExample) | 2015-07-24 |
| FR2950053B1 (fr) | 2014-08-01 |
| NZ598576A (en) | 2014-05-30 |
| TW201119650A (en) | 2011-06-16 |
| CL2012000632A1 (es) | 2012-10-19 |
| AR078358A1 (es) | 2011-11-02 |
| SG178451A1 (en) | 2012-03-29 |
| DOP2012000061A (es) | 2012-09-30 |
| EP2475642A1 (fr) | 2012-07-18 |
| AU2010294018A1 (en) | 2012-03-29 |
| SA110310698B1 (ar) | 2014-11-16 |
| CN103554006A (zh) | 2014-02-05 |
| CA2772697A1 (fr) | 2011-03-17 |
| CO6511224A2 (es) | 2012-08-31 |
| ECSP12011718A (es) | 2012-04-30 |
| FR2950058B1 (fr) | 2016-04-01 |
| CN102596906A (zh) | 2012-07-18 |
| FR2950053A1 (fr) | 2011-03-18 |
| WO2011030068A1 (fr) | 2011-03-17 |
| JP2013504548A (ja) | 2013-02-07 |
| PE20121346A1 (es) | 2012-10-15 |
| PH12012500390A1 (en) | 2012-10-22 |
| ZA201201400B (en) | 2013-05-29 |
| KR20120065345A (ko) | 2012-06-20 |
| BR112012005480A2 (pt) | 2019-09-24 |
| CR20120131A (es) | 2012-07-27 |
| FR2950058A1 (fr) | 2011-03-18 |
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