JP2008506708A5 - - Google Patents
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- Publication number
- JP2008506708A5 JP2008506708A5 JP2007521673A JP2007521673A JP2008506708A5 JP 2008506708 A5 JP2008506708 A5 JP 2008506708A5 JP 2007521673 A JP2007521673 A JP 2007521673A JP 2007521673 A JP2007521673 A JP 2007521673A JP 2008506708 A5 JP2008506708 A5 JP 2008506708A5
- Authority
- JP
- Japan
- Prior art keywords
- alkyl
- group
- aminomethyl
- phenyl
- amino
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Granted
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- 125000000217 alkyl group Chemical group 0.000 claims 119
- -1 aryl (C 1-10 ) alkyl Chemical group 0.000 claims 76
- 150000001875 compounds Chemical class 0.000 claims 58
- 125000001072 heteroaryl group Chemical group 0.000 claims 49
- 125000005842 heteroatom Chemical group 0.000 claims 46
- 125000000753 cycloalkyl group Chemical group 0.000 claims 44
- 125000002915 carbonyl group Chemical group [*:2]C([*:1])=O 0.000 claims 36
- 125000000008 (C1-C10) alkyl group Chemical group 0.000 claims 33
- 125000000475 sulfinyl group Chemical group [*:2]S([*:1])=O 0.000 claims 32
- 125000001841 imino group Chemical group [H]N=* 0.000 claims 31
- 125000000472 sulfonyl group Chemical group *S(*)(=O)=O 0.000 claims 29
- 125000003118 aryl group Chemical group 0.000 claims 28
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 27
- 125000003545 alkoxy group Chemical group 0.000 claims 20
- 125000004104 aryloxy group Chemical group 0.000 claims 19
- 229910052739 hydrogen Inorganic materials 0.000 claims 19
- 239000001257 hydrogen Substances 0.000 claims 19
- 125000002813 thiocarbonyl group Chemical group *C(*)=S 0.000 claims 18
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 17
- 125000005553 heteroaryloxy group Chemical group 0.000 claims 15
- 150000002431 hydrogen Chemical class 0.000 claims 15
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims 12
- 229940124597 therapeutic agent Drugs 0.000 claims 12
- 239000003814 drug Substances 0.000 claims 11
- 125000005843 halogen group Chemical group 0.000 claims 11
- 125000004202 aminomethyl group Chemical group [H]N([H])C([H])([H])* 0.000 claims 9
- 125000004093 cyano group Chemical group *C#N 0.000 claims 8
- 125000000592 heterocycloalkyl group Chemical group 0.000 claims 8
- 239000008194 pharmaceutical composition Substances 0.000 claims 7
- 125000004391 aryl sulfonyl group Chemical group 0.000 claims 6
- 125000003342 alkenyl group Chemical group 0.000 claims 5
- 125000004390 alkyl sulfonyl group Chemical group 0.000 claims 5
- 125000000304 alkynyl group Chemical group 0.000 claims 5
- 125000004397 aminosulfonyl group Chemical group NS(=O)(=O)* 0.000 claims 5
- 201000010099 disease Diseases 0.000 claims 5
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 5
- 108010067722 Dipeptidyl Peptidase 4 Proteins 0.000 claims 4
- 102100025012 Dipeptidyl peptidase 4 Human genes 0.000 claims 4
- 125000003710 aryl alkyl group Chemical group 0.000 claims 4
- 125000004446 heteroarylalkyl group Chemical group 0.000 claims 4
- 125000005143 heteroarylsulfonyl group Chemical group 0.000 claims 4
- 239000000203 mixture Substances 0.000 claims 4
- 125000003282 alkyl amino group Chemical group 0.000 claims 3
- JFDZBHWFFUWGJE-UHFFFAOYSA-N benzonitrile Chemical compound N#CC1=CC=CC=C1 JFDZBHWFFUWGJE-UHFFFAOYSA-N 0.000 claims 3
- 239000003112 inhibitor Substances 0.000 claims 3
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 claims 3
- 125000001424 substituent group Chemical group 0.000 claims 3
- PBOZNYRGRFQUIM-UHFFFAOYSA-N 7-amino-6-(aminomethyl)-5-(2-bromo-5-fluorophenyl)-1,3-dimethylpyrido[2,3-d]pyrimidine-2,4-dione Chemical compound C=12C(=O)N(C)C(=O)N(C)C2=NC(N)=C(CN)C=1C1=CC(F)=CC=C1Br PBOZNYRGRFQUIM-UHFFFAOYSA-N 0.000 claims 2
- 208000023275 Autoimmune disease Diseases 0.000 claims 2
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 2
- 150000001602 bicycloalkyls Chemical group 0.000 claims 2
- 125000004122 cyclic group Chemical group 0.000 claims 2
- 239000002552 dosage form Substances 0.000 claims 2
- 230000000694 effects Effects 0.000 claims 2
- 125000001475 halogen functional group Chemical group 0.000 claims 2
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims 2
- 125000004356 hydroxy functional group Chemical group O* 0.000 claims 2
- 239000012669 liquid formulation Substances 0.000 claims 2
- 229910052760 oxygen Inorganic materials 0.000 claims 2
- 239000005022 packaging material Substances 0.000 claims 2
- 229910052717 sulfur Inorganic materials 0.000 claims 2
- 125000004191 (C1-C6) alkoxy group Chemical group 0.000 claims 1
- GHNOPDKEEAXOFX-UHFFFAOYSA-N 2,7-diamino-6-(1-aminoethyl)-5-(2-chloro-5-fluorophenyl)-3-methylpyrido[2,3-d]pyrimidin-4-one Chemical compound CC(N)C1=C(N)N=C2N=C(N)N(C)C(=O)C2=C1C1=CC(F)=CC=C1Cl GHNOPDKEEAXOFX-UHFFFAOYSA-N 0.000 claims 1
- YYXIAIHZOQWCIZ-UHFFFAOYSA-N 2-[6-(aminomethyl)-1,3,7-trimethyl-2,4-dioxopyrido[2,3-d]pyrimidin-5-yl]-4-fluorobenzonitrile Chemical compound NCC=1C(C)=NC=2N(C)C(=O)N(C)C(=O)C=2C=1C1=CC(F)=CC=C1C#N YYXIAIHZOQWCIZ-UHFFFAOYSA-N 0.000 claims 1
- FOQRWMXKHJTMRG-UHFFFAOYSA-N 2-[6-(aminomethyl)-1,3-dimethyl-2,4-dioxo-7-(2,2,2-trifluoroethylamino)pyrido[2,3-d]pyrimidin-5-yl]-4-fluorobenzonitrile Chemical compound C=12C(=O)N(C)C(=O)N(C)C2=NC(NCC(F)(F)F)=C(CN)C=1C1=CC(F)=CC=C1C#N FOQRWMXKHJTMRG-UHFFFAOYSA-N 0.000 claims 1
- SBXLTVLZUDWGAH-UHFFFAOYSA-N 2-[6-(aminomethyl)-1,3-dimethyl-2,4-dioxo-7-(trifluoromethyl)pyrido[2,3-d]pyrimidin-5-yl]-4-fluorobenzonitrile Chemical compound C=12C(=O)N(C)C(=O)N(C)C2=NC(C(F)(F)F)=C(CN)C=1C1=CC(F)=CC=C1C#N SBXLTVLZUDWGAH-UHFFFAOYSA-N 0.000 claims 1
- YNCWECQLJKSAKV-UHFFFAOYSA-N 2-[6-(aminomethyl)-1,3-dimethyl-2,4-dioxo-7-pyrrolidin-1-ylpyrido[2,3-d]pyrimidin-5-yl]-5-chlorobenzonitrile Chemical compound NCC=1C(C=2C(=CC(Cl)=CC=2)C#N)=C2C(=O)N(C)C(=O)N(C)C2=NC=1N1CCCC1 YNCWECQLJKSAKV-UHFFFAOYSA-N 0.000 claims 1
- UCPJRWMTPLQOPJ-UHFFFAOYSA-N 2-[6-(aminomethyl)-1,3-dimethyl-2,4-dioxopyrido[2,3-d]pyrimidin-5-yl]-4-fluorobenzonitrile Chemical compound C=12C(=O)N(C)C(=O)N(C)C2=NC=C(CN)C=1C1=CC(F)=CC=C1C#N UCPJRWMTPLQOPJ-UHFFFAOYSA-N 0.000 claims 1
- QFDZRYGQHHPCTI-UHFFFAOYSA-N 2-[6-(aminomethyl)-3-(cyclopropylmethyl)-1,7-dimethyl-2,4-dioxopyrido[2,3-d]pyrimidin-5-yl]-5-chlorobenzonitrile Chemical compound O=C1C=2C(C=3C(=CC(Cl)=CC=3)C#N)=C(CN)C(C)=NC=2N(C)C(=O)N1CC1CC1 QFDZRYGQHHPCTI-UHFFFAOYSA-N 0.000 claims 1
- NAVFRWGPYJGCQW-UHFFFAOYSA-N 2-[6-(aminomethyl)-7-[bis(trifluoromethyl)amino]-1,3-dimethyl-2,4-dioxopyrido[2,3-d]pyrimidin-5-yl]-4-fluorobenzonitrile Chemical compound C=12C(=O)N(C)C(=O)N(C)C2=NC(N(C(F)(F)F)C(F)(F)F)=C(CN)C=1C1=CC(F)=CC=C1C#N NAVFRWGPYJGCQW-UHFFFAOYSA-N 0.000 claims 1
- SGGHBAVUMJDAEM-UHFFFAOYSA-N 2-[6-(aminomethyl)-7-chloro-1,3-dimethyl-2,4-dioxopyrido[2,3-d]pyrimidin-5-yl]-4-fluorobenzonitrile Chemical compound C=12C(=O)N(C)C(=O)N(C)C2=NC(Cl)=C(CN)C=1C1=CC(F)=CC=C1C#N SGGHBAVUMJDAEM-UHFFFAOYSA-N 0.000 claims 1
- PTUZDYBWBWNURF-UHFFFAOYSA-N 2-[6-(aminomethyl)-7-ethoxy-1,3-dimethyl-2,4-dioxopyrido[2,3-d]pyrimidin-5-yl]-5-chlorobenzonitrile Chemical compound NCC=1C(OCC)=NC=2N(C)C(=O)N(C)C(=O)C=2C=1C1=CC=C(Cl)C=C1C#N PTUZDYBWBWNURF-UHFFFAOYSA-N 0.000 claims 1
- ZSXQRILDNYNHAX-UHFFFAOYSA-N 2-[6-(aminomethyl)-7-methoxy-1,3-dimethyl-2,4-dioxopyrido[2,3-d]pyrimidin-5-yl]-5-chlorobenzonitrile Chemical compound NCC=1C(OC)=NC=2N(C)C(=O)N(C)C(=O)C=2C=1C1=CC=C(Cl)C=C1C#N ZSXQRILDNYNHAX-UHFFFAOYSA-N 0.000 claims 1
- VFPBKHMUTLLLAE-UHFFFAOYSA-N 2-[7-amino-6-(aminomethyl)-1,3-dimethyl-2,4-dioxopyrido[2,3-d]pyrimidin-5-yl]-4-fluorobenzonitrile Chemical compound C=12C(=O)N(C)C(=O)N(C)C2=NC(N)=C(CN)C=1C1=CC(F)=CC=C1C#N VFPBKHMUTLLLAE-UHFFFAOYSA-N 0.000 claims 1
- BPVOKDDONNBGTD-UHFFFAOYSA-N 2-[7-amino-6-(aminomethyl)-1,3-dimethyl-2,4-dioxopyrido[2,3-d]pyrimidin-5-yl]benzonitrile Chemical compound C=12C(=O)N(C)C(=O)N(C)C2=NC(N)=C(CN)C=1C1=CC=CC=C1C#N BPVOKDDONNBGTD-UHFFFAOYSA-N 0.000 claims 1
- IGLZUUDBLGOTDT-UHFFFAOYSA-N 5-(2-bromo-5-fluorophenyl)-1,3-dimethyl-2,4,7-trioxo-8h-pyrido[2,3-d]pyrimidine-6-carbonitrile Chemical compound C=12C(=O)N(C)C(=O)N(C)C2=NC(O)=C(C#N)C=1C1=CC(F)=CC=C1Br IGLZUUDBLGOTDT-UHFFFAOYSA-N 0.000 claims 1
- LNLBAJHYXLTXRD-UHFFFAOYSA-N 5-(2-bromo-5-fluorophenyl)-1,3-dimethyl-7-morpholin-4-yl-2,4-dioxopyrido[2,3-d]pyrimidine-6-carbonitrile Chemical compound N#CC=1C(C=2C(=CC=C(F)C=2)Br)=C2C(=O)N(C)C(=O)N(C)C2=NC=1N1CCOCC1 LNLBAJHYXLTXRD-UHFFFAOYSA-N 0.000 claims 1
- ITURIGSYOOMUAV-UHFFFAOYSA-N 5-(2-bromo-5-fluorophenyl)-7-chloro-1,3-dimethyl-2,4-dioxopyrido[2,3-d]pyrimidine-6-carbonitrile Chemical compound C=12C(=O)N(C)C(=O)N(C)C2=NC(Cl)=C(C#N)C=1C1=CC(F)=CC=C1Br ITURIGSYOOMUAV-UHFFFAOYSA-N 0.000 claims 1
- VFPRFVSEPLFKAI-UHFFFAOYSA-N 6-(aminomethyl)-3-benzyl-5-(2-chloro-3,5-difluorophenyl)-1-methyl-7-(trifluoromethyl)pyrido[2,3-d]pyrimidine-2,4-dione Chemical compound C=12C(=O)N(CC=3C=CC=CC=3)C(=O)N(C)C2=NC(C(F)(F)F)=C(CN)C=1C1=CC(F)=CC(F)=C1Cl VFPRFVSEPLFKAI-UHFFFAOYSA-N 0.000 claims 1
- KLZQPRPXUFHTTA-UHFFFAOYSA-N 6-(aminomethyl)-3-benzyl-5-(4-chloro-2-methoxyphenyl)-1-methyl-7-(trifluoromethyl)pyrido[2,3-d]pyrimidine-2,4-dione Chemical compound COC1=CC(Cl)=CC=C1C1=C(CN)C(C(F)(F)F)=NC2=C1C(=O)N(CC=1C=CC=CC=1)C(=O)N2C KLZQPRPXUFHTTA-UHFFFAOYSA-N 0.000 claims 1
- FLOKCOVNZXIQPN-UHFFFAOYSA-N 6-(aminomethyl)-5-(2,4-dichlorophenyl)-1,3-dimethyl-7-(methylamino)pyrido[2,3-d]pyrimidine-2,4-dione Chemical compound NCC=1C(NC)=NC=2N(C)C(=O)N(C)C(=O)C=2C=1C1=CC=C(Cl)C=C1Cl FLOKCOVNZXIQPN-UHFFFAOYSA-N 0.000 claims 1
- MCNSYOCSWOKACY-UHFFFAOYSA-N 6-(aminomethyl)-5-(2,4-dichlorophenyl)-1,3-dimethyl-8h-pyrido[2,3-d]pyrimidine-2,4,7-trione Chemical compound C=12C(=O)N(C)C(=O)N(C)C2=NC(O)=C(CN)C=1C1=CC=C(Cl)C=C1Cl MCNSYOCSWOKACY-UHFFFAOYSA-N 0.000 claims 1
- ROJWXYBULXPBKW-UHFFFAOYSA-N 6-(aminomethyl)-5-(2,4-dichlorophenyl)-1,3-dimethylpyrido[2,3-d]pyrimidine-2,4-dione Chemical compound C=12C(=O)N(C)C(=O)N(C)C2=NC=C(CN)C=1C1=CC=C(Cl)C=C1Cl ROJWXYBULXPBKW-UHFFFAOYSA-N 0.000 claims 1
- QXVLCIVEIASULH-UHFFFAOYSA-N 6-(aminomethyl)-5-(2,4-dichlorophenyl)-7-(dimethylamino)-1,3-dimethylpyrido[2,3-d]pyrimidine-2,4-dione Chemical compound NCC=1C(N(C)C)=NC=2N(C)C(=O)N(C)C(=O)C=2C=1C1=CC=C(Cl)C=C1Cl QXVLCIVEIASULH-UHFFFAOYSA-N 0.000 claims 1
- YOJMMUNVHSHXMC-UHFFFAOYSA-N 6-(aminomethyl)-5-(2,4-dichlorophenyl)-7-(ethylamino)-1,3-dimethylpyrido[2,3-d]pyrimidine-2,4-dione Chemical compound NCC=1C(NCC)=NC=2N(C)C(=O)N(C)C(=O)C=2C=1C1=CC=C(Cl)C=C1Cl YOJMMUNVHSHXMC-UHFFFAOYSA-N 0.000 claims 1
- IDKCTEQTCQCYNX-UHFFFAOYSA-N 6-(aminomethyl)-5-(2-bromo-3,5-difluorophenyl)-1,3-dimethyl-7-(trifluoromethyl)pyrido[2,3-d]pyrimidine-2,4-dione Chemical compound C=12C(=O)N(C)C(=O)N(C)C2=NC(C(F)(F)F)=C(CN)C=1C1=CC(F)=CC(F)=C1Br IDKCTEQTCQCYNX-UHFFFAOYSA-N 0.000 claims 1
- PPJPCHRLGTVRBJ-UHFFFAOYSA-N 6-(aminomethyl)-5-(2-bromo-5-fluorophenyl)-1,3-dimethyl-7-(4-methylpiperazin-1-yl)pyrido[2,3-d]pyrimidine-2,4-dione Chemical compound C1CN(C)CCN1C(C(=C1C=2C(=CC=C(F)C=2)Br)CN)=NC2=C1C(=O)N(C)C(=O)N2C PPJPCHRLGTVRBJ-UHFFFAOYSA-N 0.000 claims 1
- VDWGTMUMUISEGS-UHFFFAOYSA-N 6-(aminomethyl)-5-(2-bromo-5-fluorophenyl)-1,3-dimethyl-7-(methylamino)pyrido[2,3-d]pyrimidine-2,4-dione Chemical compound NCC=1C(NC)=NC=2N(C)C(=O)N(C)C(=O)C=2C=1C1=CC(F)=CC=C1Br VDWGTMUMUISEGS-UHFFFAOYSA-N 0.000 claims 1
- CXIIQRMCLKMMJF-UHFFFAOYSA-N 6-(aminomethyl)-5-(2-bromo-5-fluorophenyl)-1,3-dimethyl-7-(pyridin-4-ylmethylamino)pyrido[2,3-d]pyrimidine-2,4-dione Chemical compound NCC=1C(C=2C(=CC=C(F)C=2)Br)=C2C(=O)N(C)C(=O)N(C)C2=NC=1NCC1=CC=NC=C1 CXIIQRMCLKMMJF-UHFFFAOYSA-N 0.000 claims 1
- PTGQTILYRYFWNL-UHFFFAOYSA-N 6-(aminomethyl)-5-(2-bromo-5-fluorophenyl)-1,3-dimethyl-7-morpholin-4-ylpyrido[2,3-d]pyrimidine-2,4-dione Chemical compound NCC=1C(C=2C(=CC=C(F)C=2)Br)=C2C(=O)N(C)C(=O)N(C)C2=NC=1N1CCOCC1 PTGQTILYRYFWNL-UHFFFAOYSA-N 0.000 claims 1
- UHYAYBQYODCACG-UHFFFAOYSA-N 6-(aminomethyl)-5-(2-bromo-5-fluorophenyl)-1,3-dimethyl-8h-pyrido[2,3-d]pyrimidine-2,4,7-trione Chemical compound C=12C(=O)N(C)C(=O)N(C)C2=NC(O)=C(CN)C=1C1=CC(F)=CC=C1Br UHYAYBQYODCACG-UHFFFAOYSA-N 0.000 claims 1
- KWUIPYRTIGQIQH-UHFFFAOYSA-N 6-(aminomethyl)-5-(2-bromo-5-fluorophenyl)-7-(diethylamino)-1,3-dimethylpyrido[2,3-d]pyrimidine-2,4-dione Chemical compound NCC=1C(N(CC)CC)=NC=2N(C)C(=O)N(C)C(=O)C=2C=1C1=CC(F)=CC=C1Br KWUIPYRTIGQIQH-UHFFFAOYSA-N 0.000 claims 1
- PXXXJKLIYAELBV-UHFFFAOYSA-N 6-(aminomethyl)-5-(2-bromo-5-fluorophenyl)-7-(ethylamino)-1,3-dimethylpyrido[2,3-d]pyrimidine-2,4-dione Chemical compound NCC=1C(NCC)=NC=2N(C)C(=O)N(C)C(=O)C=2C=1C1=CC(F)=CC=C1Br PXXXJKLIYAELBV-UHFFFAOYSA-N 0.000 claims 1
- LSLOGTFSQHTFRR-UHFFFAOYSA-N 6-(aminomethyl)-5-(3,5-difluoro-2-methoxyphenyl)-1,3-dimethyl-7-(trifluoromethyl)pyrido[2,3-d]pyrimidine-2,4-dione Chemical compound COC1=C(F)C=C(F)C=C1C1=C(CN)C(C(F)(F)F)=NC2=C1C(=O)N(C)C(=O)N2C LSLOGTFSQHTFRR-UHFFFAOYSA-N 0.000 claims 1
- KWYFMUCKFHCEFP-UHFFFAOYSA-N 6-(aminomethyl)-5-(3,5-difluoro-2-methoxyphenyl)-2-(dimethylamino)-3-methyl-7-(trifluoromethyl)pyrido[2,3-d]pyrimidin-4-one Chemical compound COC1=C(F)C=C(F)C=C1C1=C(CN)C(C(F)(F)F)=NC2=C1C(=O)N(C)C(N(C)C)=N2 KWYFMUCKFHCEFP-UHFFFAOYSA-N 0.000 claims 1
- YVKBGMDKVVVPBK-UHFFFAOYSA-N 6-(aminomethyl)-5-(3,5-difluoro-2-methoxyphenyl)-3-methyl-2-(methylamino)-7-(trifluoromethyl)pyrido[2,3-d]pyrimidin-4-one Chemical compound C=12C(=O)N(C)C(NC)=NC2=NC(C(F)(F)F)=C(CN)C=1C1=CC(F)=CC(F)=C1OC YVKBGMDKVVVPBK-UHFFFAOYSA-N 0.000 claims 1
- AZMCIAMRJIHRFZ-UHFFFAOYSA-N 6-(aminomethyl)-5-(4-chloro-2-methoxyphenyl)-1,3,7-trimethylpyrido[2,3-d]pyrimidine-2,4-dione Chemical compound COC1=CC(Cl)=CC=C1C1=C(CN)C(C)=NC2=C1C(=O)N(C)C(=O)N2C AZMCIAMRJIHRFZ-UHFFFAOYSA-N 0.000 claims 1
- ABANWMZTDDAKEH-UHFFFAOYSA-N 6-(aminomethyl)-5-(5-fluoro-2-methoxyphenyl)-1,3-dimethyl-7-morpholin-4-ylpyrido[2,3-d]pyrimidine-2,4-dione Chemical compound COC1=CC=C(F)C=C1C1=C(CN)C(N2CCOCC2)=NC2=C1C(=O)N(C)C(=O)N2C ABANWMZTDDAKEH-UHFFFAOYSA-N 0.000 claims 1
- JQQOLNZRFCWMRZ-UHFFFAOYSA-N 6-(aminomethyl)-7-(cyclopropylmethylamino)-5-(2,4-dichlorophenyl)-1,3-dimethylpyrido[2,3-d]pyrimidine-2,4-dione Chemical compound NCC=1C(C=2C(=CC(Cl)=CC=2)Cl)=C2C(=O)N(C)C(=O)N(C)C2=NC=1NCC1CC1 JQQOLNZRFCWMRZ-UHFFFAOYSA-N 0.000 claims 1
- WFTDPRDHZSJQCE-UHFFFAOYSA-N 6-(aminomethyl)-7-[bis(2,2-difluoroethyl)amino]-5-(2-bromo-5-fluorophenyl)-1,3-dimethylpyrido[2,3-d]pyrimidine-2,4-dione Chemical compound C=12C(=O)N(C)C(=O)N(C)C2=NC(N(CC(F)F)CC(F)F)=C(CN)C=1C1=CC(F)=CC=C1Br WFTDPRDHZSJQCE-UHFFFAOYSA-N 0.000 claims 1
- UYLKKDOQGIKGFR-UHFFFAOYSA-N 6-(aminomethyl)-7-chloro-5-(2,4-dichlorophenyl)-1,3-dimethylpyrido[2,3-d]pyrimidine-2,4-dione Chemical compound C=12C(=O)N(C)C(=O)N(C)C2=NC(Cl)=C(CN)C=1C1=CC=C(Cl)C=C1Cl UYLKKDOQGIKGFR-UHFFFAOYSA-N 0.000 claims 1
- AUGQLMNHLALSNI-UHFFFAOYSA-N 7-amino-5-(2,5-dichlorophenyl)-1,3-dimethyl-2,4-dioxopyrido[2,3-d]pyrimidine-6-carbonitrile Chemical compound C=12C(=O)N(C)C(=O)N(C)C2=NC(N)=C(C#N)C=1C1=CC(Cl)=CC=C1Cl AUGQLMNHLALSNI-UHFFFAOYSA-N 0.000 claims 1
- IVZLPHVERJFCTF-UHFFFAOYSA-N 7-amino-5-[2-(aminomethyl)phenyl]-1,3-dimethyl-2,4-dioxopyrido[2,3-d]pyrimidine-6-carbonitrile Chemical compound C=12C(=O)N(C)C(=O)N(C)C2=NC(N)=C(C#N)C=1C1=CC=CC=C1CN IVZLPHVERJFCTF-UHFFFAOYSA-N 0.000 claims 1
- YEWACWFQUSSPGZ-UHFFFAOYSA-N 7-amino-6-(aminomethyl)-1,3-dimethyl-5-(3-methyl-1-benzothiophen-2-yl)pyrido[2,3-d]pyrimidine-2,4-dione Chemical compound CN1C(=O)N(C)C(=O)C2=C1N=C(N)C(CN)=C2C1=C(C)C2=CC=CC=C2S1 YEWACWFQUSSPGZ-UHFFFAOYSA-N 0.000 claims 1
- HEMHQMJOXSBMLV-UHFFFAOYSA-N 7-amino-6-(aminomethyl)-1,3-dimethyl-5-(3-methylimidazol-4-yl)pyrido[2,3-d]pyrimidine-2,4-dione Chemical compound CN1C=NC=C1C1=C(CN)C(N)=NC2=C1C(=O)N(C)C(=O)N2C HEMHQMJOXSBMLV-UHFFFAOYSA-N 0.000 claims 1
- QVTZKWQWDHVEQE-UHFFFAOYSA-N 7-amino-6-(aminomethyl)-1,3-dimethyl-5-(3-methylthiophen-2-yl)pyrido[2,3-d]pyrimidine-2,4-dione Chemical compound C1=CSC(C=2C=3C(=O)N(C)C(=O)N(C)C=3N=C(N)C=2CN)=C1C QVTZKWQWDHVEQE-UHFFFAOYSA-N 0.000 claims 1
- LAMTXHIPLANNMZ-UHFFFAOYSA-N 7-amino-6-(aminomethyl)-1,3-dimethyl-5-phenylpyrido[2,3-d]pyrimidine-2,4-dione Chemical compound C=12C(=O)N(C)C(=O)N(C)C2=NC(N)=C(CN)C=1C1=CC=CC=C1 LAMTXHIPLANNMZ-UHFFFAOYSA-N 0.000 claims 1
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| JP5934645B2 (ja) | 2009-09-11 | 2016-06-15 | プロビオドルグ エージー | グルタミニルシクラーゼ阻害剤としてのヘテロ環式誘導体 |
| JP6026284B2 (ja) | 2010-03-03 | 2016-11-16 | プロビオドルグ エージー | グルタミニルシクラーゼの阻害剤 |
| NZ602312A (en) | 2010-03-10 | 2014-02-28 | Probiodrug Ag | Heterocyclic inhibitors of glutaminyl cyclase (qc, ec 2.3.2.5) |
| WO2011131748A2 (en) | 2010-04-21 | 2011-10-27 | Probiodrug Ag | Novel inhibitors |
| WO2011143521A2 (en) * | 2010-05-13 | 2011-11-17 | Dara Biosciences, Inc. | Enhanced homing and engraftment of hematopoietic stem cells using cd26 inhibitors |
| EP2582673B1 (de) * | 2010-06-15 | 2014-08-06 | Bayer Intellectual Property GmbH | Verfahren zur herstellung von 2,2-difluorethylamin-derivaten durch alkylierung mit 2,2- difluor-1-halogenethanen |
| EP2680851B1 (en) | 2011-03-03 | 2016-08-17 | Merck Sharp & Dohme Corp. | Fused bicyclic heterocycles useful as dipeptidyl peptidase-iv inhibitors |
| EP2686313B1 (en) | 2011-03-16 | 2016-02-03 | Probiodrug AG | Benzimidazole derivatives as inhibitors of glutaminyl cyclase |
| EA201791982A1 (ru) | 2015-03-09 | 2020-02-17 | Интекрин Терапьютикс, Инк. | Способы лечения неалкогольной жировой болезни печени и/или липодистрофии |
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| JP2020515639A (ja) | 2017-04-03 | 2020-05-28 | コヒラス・バイオサイエンシズ・インコーポレイテッド | 進行性核上性麻痺の処置のためのＰＰＡＲγアゴニスト |
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| US10100054B1 (en) | 2018-04-03 | 2018-10-16 | King Saud University | Pyrido[2,3-d]pyrimidines as anticancer agents |
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-
2005
- 2005-07-14 WO PCT/US2005/025070 patent/WO2006019965A2/en not_active Ceased
- 2005-07-15 WO PCT/US2005/025153 patent/WO2006020017A2/en not_active Ceased
- 2005-07-15 EP EP05772260A patent/EP1773832A2/en not_active Withdrawn
- 2005-07-15 JP JP2007521673A patent/JP4945443B2/ja not_active Expired - Fee Related
- 2005-07-15 US US11/183,335 patent/US7825242B2/en not_active Expired - Fee Related
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