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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| JP5945532B2 (ja) | 2010-04-21 | 2016-07-05 | 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としてのベンゾイミダゾール誘導体 |
| WO2011143521A2 (en) * | 2010-05-13 | 2011-11-17 | Dara Biosciences, Inc. | Enhanced homing and engraftment of hematopoietic stem cells using cd26 inhibitors |
| KR101790159B1 (ko) * | 2010-06-15 | 2017-10-25 | 바이엘 인텔렉쳐 프로퍼티 게엠베하 | 2,2-디플루오로-1-할로에탄의 알킬화에 의한 2,2-디플루오로에틸아민 유도체의 제조 방법 |
| EP2680851B1 (en) | 2011-03-03 | 2016-08-17 | Merck Sharp & Dohme Corp. | Fused bicyclic heterocycles useful as dipeptidyl peptidase-iv inhibitors |
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| MX386778B (es) | 2015-03-09 | 2025-03-19 | Intekrin Therapeutics Inc | Métodos para el tratamiento de enfermedad de hígado graso no alcohólico y/o lipodistrofia. |
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| US10100054B1 (en) | 2018-04-03 | 2018-10-16 | King Saud University | Pyrido[2,3-d]pyrimidines as anticancer agents |
Family Cites Families (255)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US2961377A (en) | 1957-08-05 | 1960-11-22 | Us Vitamin Pharm Corp | Oral anti-diabetic compositions and methods |
| US3947442A (en) * | 1969-11-20 | 1976-03-30 | The Sherwin-Williams Company | Method for producing heterocyclic acid anhydrides and pyrimidinediones |
| US3960949A (en) | 1971-04-02 | 1976-06-01 | Schering Aktiengesellschaft | 1,2-Biguanides |
| US4113859A (en) * | 1972-10-12 | 1978-09-12 | Burroughs Wellcome Co. | Certain pyrido-pyrimidines for treating mammalian and avian infections |
| US3922275A (en) * | 1972-11-09 | 1975-11-25 | Hisamitsu Pharmaceutical Co | Pyrido{8 2,3-D{9 {0 pyrimidine-2,4(1H,3H)-diones |
| US4494978A (en) | 1976-12-30 | 1985-01-22 | Chevron Research Company | Herbicidal N-(N'-hydrocarbyloxycarbamylalkyl)-2,6-dialkyl-alpha-haloacetanilides |
| US4808587A (en) * | 1986-04-16 | 1989-02-28 | Nippon Zoki Pharmaceutical Co., Ltd. | 5-substituted pyrido[2,3-d]pyrimidine-2,4-diones |
| ES2031513T3 (es) * | 1986-08-21 | 1992-12-16 | Pfizer Inc. | Quinazolindionas y piridopirimidinadionas. |
| US4935493A (en) | 1987-10-06 | 1990-06-19 | E. I. Du Pont De Nemours And Company | Protease inhibitors |
| AU618158B2 (en) * | 1989-01-07 | 1991-12-12 | Bayer Aktiengesellschaft | New substituted pyrido(2,3-d)pyrimidines |
| US5433955A (en) | 1989-01-23 | 1995-07-18 | Akzo N.V. | Site specific in vivo activation of therapeutic drugs |
| US5814460A (en) | 1990-02-14 | 1998-09-29 | Diatide, Inc. | Method for generating and screening useful peptides |
| US5366862A (en) | 1990-02-14 | 1994-11-22 | Receptor Laboratories, Inc. | Method for generating and screening useful peptides |
| US5462928A (en) | 1990-04-14 | 1995-10-31 | New England Medical Center Hospitals, Inc. | Inhibitors of dipeptidyl-aminopeptidase type IV |
| DE4110019C2 (de) | 1991-03-27 | 2000-04-13 | Merck Patent Gmbh | Imidazopyridine, Verfahren zu ihrer Herstellung und diese enthaltende pharmazeutische Zubereitungen |
| US5387512A (en) | 1991-06-07 | 1995-02-07 | Merck & Co. Inc. | Preparation of 3-[z-benzoxazol-2-yl)ethyl]-5-(1-hydroxyethyl)-6-methyl-2-(1H)-pyridinone by biotransformation |
| US5268376A (en) | 1991-09-04 | 1993-12-07 | Minnesota Mining And Manufacturing Company | 1-substituted 1H-imidazo[4,5-c]quinolin-4-amines |
| US6825169B1 (en) | 1991-10-22 | 2004-11-30 | Trustees Of Tufts College | Inhibitors of dipeptidyl-aminopeptidase type IV |
| EP1050540B1 (en) | 1991-10-22 | 2006-12-27 | New England Medical Center Hospitals, Inc. | Inhibitors of dipeptidyl-aminopeptidase type IV |
| US5342843A (en) | 1991-12-12 | 1994-08-30 | Kyowa Hakko Kogyo Co., Ltd. | Thienoimidazoppyridone derivatives |
| DE4141788A1 (de) | 1991-12-18 | 1993-06-24 | Merck Patent Gmbh | Imidazopyridine |
| US5264437A (en) * | 1992-03-20 | 1993-11-23 | Syntex (U.S.A.) Inc. | Optionally substituted pyrido[2,3-d]pyridine-2,4(1H,3H)-diones and pyrido[2,]pyrimidine-2(1H,3H)-ones |
| DE4305602A1 (de) | 1992-06-17 | 1993-12-23 | Merck Patent Gmbh | Imidazopyridine |
| IL106998A0 (en) | 1992-09-17 | 1993-12-28 | Univ Florida | Brain-enhanced delivery of neuroactive peptides by sequential metabolism |
| TW299333B (enExample) * | 1992-12-29 | 1997-03-01 | Takeda Pharm Industry Co Ltd | |
| US5811281A (en) | 1993-07-12 | 1998-09-22 | Cornell Research Foundation, Inc. | Immortalized intestinal epithelial cell lines |
| IL111785A0 (en) | 1993-12-03 | 1995-01-24 | Ferring Bv | Dp-iv inhibitors and pharmaceutical compositions containing them |
| DE4341453A1 (de) | 1993-12-06 | 1995-06-08 | Merck Patent Gmbh | Imidazopyridine |
| KR100233703B1 (ko) | 1994-03-08 | 1999-12-01 | 오츠까 요시미쯔 | 포스폰산 디에스테르 유도체 |
| US5580979A (en) | 1994-03-15 | 1996-12-03 | Trustees Of Tufts University | Phosphotyrosine peptidomimetics for inhibiting SH2 domain interactions |
| US5543396A (en) | 1994-04-28 | 1996-08-06 | Georgia Tech Research Corp. | Proline phosphonate derivatives |
| AU2790895A (en) | 1994-06-10 | 1996-01-05 | Universitaire Instelling Antwerpen | Purification of serine protease and synthetic inhibitors thereof |
| US5589437A (en) | 1994-06-13 | 1996-12-31 | Vichnevetskaia; Klara D. | Method of using 5-hydroxybenzimidazole compounds for reducing transpiration in plants |
| US5601986A (en) | 1994-07-14 | 1997-02-11 | Amgen Inc. | Assays and devices for the detection of extrahepatic biliary atresia |
| DE4432860A1 (de) | 1994-09-15 | 1996-03-21 | Merck Patent Gmbh | Imidazopyridine |
| US5512549A (en) | 1994-10-18 | 1996-04-30 | Eli Lilly And Company | Glucagon-like insulinotropic peptide analogs, compositions, and methods of use |
| US5614379A (en) | 1995-04-26 | 1997-03-25 | Eli Lilly And Company | Process for preparing anti-obesity protein |
| US6265551B1 (en) | 1995-06-01 | 2001-07-24 | Dana-Farber Cancer Institute, Inc. | Form of dipeptidylpeptidase IV (CD26) found in human serum, antibodies thereto, and uses thereof |
| US6325989B1 (en) | 1995-06-01 | 2001-12-04 | Dana-Farber Cancer Institute, Inc. | Form of dipeptidylpeptidase IV (CD26) found in human serum |
| JPH0928376A (ja) | 1995-07-21 | 1997-02-04 | Ajinomoto Co Inc | 新規ジペプチジルペプチダーゼｉｖとその製造方法 |
| US20020006899A1 (en) | 1998-10-06 | 2002-01-17 | Pospisilik Andrew J. | Use of dipeptidyl peptidase IV effectors for lowering blood pressure in mammals |
| DE122010000020I1 (de) | 1996-04-25 | 2010-07-08 | Prosidion Ltd | Verfahren zur Senkung des Blutglukosespiegels in Säugern |
| US6875769B2 (en) * | 1996-05-23 | 2005-04-05 | Pfizer Inc. | Substituted6,6-hetero-bicyclicderivatives |
| US5965532A (en) | 1996-06-28 | 1999-10-12 | Trustees Of Tufts College | Multivalent compounds for crosslinking receptors and uses thereof |
| CZ298812B6 (cs) | 1996-07-01 | 2008-02-13 | Dr. Reddy's Laboratories Limited | Azolidindionové deriváty, způsob jejich přípravy, farmaceutické kompozice s jejich obsahem a jejich použití v léčbě diabetu a příbuzných nemocí |
| US5885997A (en) | 1996-07-01 | 1999-03-23 | Dr. Reddy's Research Foundation | Heterocyclic compounds, process for their preparation and pharmaceutical compositions containing them and their use in the treatment of diabetes and related diseases |
| US7235627B2 (en) | 1996-08-30 | 2007-06-26 | Novo Nordisk A/S | Derivatives of GLP-1 analogs |
| US6006753A (en) | 1996-08-30 | 1999-12-28 | Eli Lilly And Company | Use of GLP-1 or analogs to abolish catabolic changes after surgery |
| US6458924B2 (en) | 1996-08-30 | 2002-10-01 | Novo Nordisk A/S | Derivatives of GLP-1 analogs |
| UA65549C2 (uk) | 1996-11-05 | 2004-04-15 | Елі Ліллі Енд Компані | Спосіб регулювання ожиріння шляхом периферійного введення аналогів та похідних glp-1 (варіанти) та фармацевтична композиція |
| US6011155A (en) | 1996-11-07 | 2000-01-04 | Novartis Ag | N-(substituted glycyl)-2-cyanopyrrolidines, pharmaceutical compositions containing them and their use in inhibiting dipeptidyl peptidase-IV |
| GB9702701D0 (en) | 1997-02-01 | 1997-04-02 | Univ Newcastle Ventures Ltd | Quinazolinone compounds |
| US6100234A (en) | 1997-05-07 | 2000-08-08 | Tufts University | Treatment of HIV |
| JP4050329B2 (ja) | 1997-05-16 | 2008-02-20 | ノボザイムス，インコーポレイテッド | プロリルピペプチジルアミノペプチダーゼ活性を有するポリペプチド及びそれをコードする核酸 |
| EP0897012A1 (en) | 1997-07-05 | 1999-02-17 | Societe Des Produits Nestle S.A. | Cloning of the prolyl-dipeptidyl-peptidase from aspergillus oryzae |
| US6235493B1 (en) | 1997-08-06 | 2001-05-22 | The Regents Of The University Of California | Amino acid substituted-cresyl violet, synthetic fluorogenic substrates for the analysis of agents in individual in vivo cells or tissue |
| CN1163594C (zh) | 1997-09-29 | 2004-08-25 | 尖端医疗有限公司 | 体外造血细胞的刺激 |
| US6485955B1 (en) | 1997-10-06 | 2002-11-26 | The Trustees Of Tufts University | Quiescent cell dipeptidyl peptidase: a novel cytoplasmic serine protease |
| US6342611B1 (en) | 1997-10-10 | 2002-01-29 | Cytovia, Inc. | Fluorogenic or fluorescent reporter molecules and their applications for whole-cell fluorescence screening assays for capsases and other enzymes and the use thereof |
| ATE239000T1 (de) * | 1997-10-28 | 2003-05-15 | Warner Lambert Co | 7-substituierte chinazolin-2,4-dionen verwendbar als antibakterielle mittel |
| US6380357B2 (en) | 1997-12-16 | 2002-04-30 | Eli Lilly And Company | Glucagon-like peptide-1 crystals |
| EP1042457B1 (en) | 1997-12-16 | 2006-03-08 | Novozymes A/S | Polypeptides having aminopeptidase activity and nucleic acids encoding same |
| DE04029691T1 (de) | 1998-02-02 | 2007-11-08 | Trustees Of Tufts College, Medford | Verwendung von Dipetidylpeptidasehemmer zur Regulierung des Glukosemetabolismus |
| US20020061839A1 (en) | 1998-03-09 | 2002-05-23 | Scharpe Simon Lodewijk | Serine peptidase modulators |
| FR2777283B1 (fr) | 1998-04-10 | 2000-11-24 | Adir | Nouveaux composes peptidiques analogues du glucagon-peptide- 1 (7-37), leur procede de preparation et les compositions pharmaceutiques qui les contiennent |
| AU770319C (en) | 1998-05-04 | 2004-11-25 | Point Therapeutics, Inc. | Hematopoietic stimulation |
| DE19823831A1 (de) | 1998-05-28 | 1999-12-02 | Probiodrug Ges Fuer Arzneim | Neue pharmazeutische Verwendung von Isoleucyl Thiazolidid und seinen Salzen |
| JP2002517401A (ja) | 1998-06-05 | 2002-06-18 | ポイント セラピューティクス， インコーポレイテッド | 環状ボロプロリン化合物 |
| DE19828113A1 (de) | 1998-06-24 | 2000-01-05 | Probiodrug Ges Fuer Arzneim | Prodrugs von Inhibitoren der Dipeptidyl Peptidase IV |
| DE19828114A1 (de) | 1998-06-24 | 2000-01-27 | Probiodrug Ges Fuer Arzneim | Produgs instabiler Inhibitoren der Dipeptidyl Peptidase IV |
| US6129911A (en) | 1998-07-10 | 2000-10-10 | Rhode Island Hospital, A Lifespan Partner | Liver stem cell |
| DE19834591A1 (de) | 1998-07-31 | 2000-02-03 | Probiodrug Ges Fuer Arzneim | Verfahren zur Steigerung des Blutglukosespiegels in Säugern |
| US20030176357A1 (en) | 1998-10-06 | 2003-09-18 | Pospisilik Andrew J. | Dipeptidyl peptidase IV inhibitors and their uses for lowering blood pressure levels |
| DE19847690A1 (de) | 1998-10-15 | 2000-04-20 | Brahms Diagnostica Gmbh | Verfahren und Substanzen für die Diagnose und Therapie von Sepsis und sepsisähnlichen systemischen Infektionen |
| JP2000119272A (ja) * | 1998-10-15 | 2000-04-25 | Nippon Zoki Pharmaceut Co Ltd | 新規７−アミノピリド〔２，３−ｄ〕ピリミジン誘導体 |
| CO5150173A1 (es) | 1998-12-10 | 2002-04-29 | Novartis Ag | Compuestos n-(glicilo sustituido)-2-cianopirrolidinas inhibidores de peptidasa de dipeptidilo-iv (dpp-iv) los cuales son efectivos en el tratamiento de condiciones mediadas por la inhibicion de dpp-iv |
| GB9906715D0 (en) | 1999-03-23 | 1999-05-19 | Ferring Bv | Compositions for promoting growth |
| US6548529B1 (en) | 1999-04-05 | 2003-04-15 | Bristol-Myers Squibb Company | Heterocyclic containing biphenyl aP2 inhibitors and method |
| AU3958100A (en) | 1999-04-20 | 2000-11-02 | Novo Nordisk A/S | New compounds, their preparation and use |
| US6358948B1 (en) | 1999-05-04 | 2002-03-19 | American Home Products Corporation | Quinazolinone and benzoxazine derivatives as progesterone receptor modulators |
| US6613879B1 (en) | 1999-05-14 | 2003-09-02 | Boehringer Ingelheim Pharma Kg | FAP-activated anti-tumour compounds |
| DE19926233C1 (de) | 1999-06-10 | 2000-10-19 | Probiodrug Ges Fuer Arzneim | Verfahren zur Herstellung von Thiazolidin |
| EP1133312B8 (en) | 1999-06-21 | 2007-10-17 | Eli Lilly And Company | Synergistic use of thiazolidinediones with glucagon-like peptide-1 and agonists thereof to treat non-insulin dependent diabetes |
| US6172081B1 (en) | 1999-06-24 | 2001-01-09 | Novartis Ag | Tetrahydroisoquinoline 3-carboxamide derivatives |
| US6107317A (en) | 1999-06-24 | 2000-08-22 | Novartis Ag | N-(substituted glycyl)-thiazolidines, pharmaceutical compositions containing them and their use in inhibiting dipeptidyl peptidase-IV |
| US6110949A (en) | 1999-06-24 | 2000-08-29 | Novartis Ag | N-(substituted glycyl)-4-cyanothiazolidines, pharmaceutical compositions containing them and their use in inhibiting dipeptidyl peptidase-IV |
| US6528486B1 (en) | 1999-07-12 | 2003-03-04 | Zealand Pharma A/S | Peptide agonists of GLP-1 activity |
| US6617340B1 (en) | 1999-07-29 | 2003-09-09 | Novartis Ag | N-(substituted glycyl)-pyrrolidines, pharmaceutical compositions containing them and their use in inhibiting dipeptidyl peptidase-IV |
| DE19940130A1 (de) | 1999-08-24 | 2001-03-01 | Probiodrug Ges Fuer Arzneim | Neue Effektoren der Dipeptidyl Peptidase IV zur topischen Anwendung |
| US6881564B1 (en) | 1999-09-10 | 2005-04-19 | The University Of Sydney | Dipeptidyl peptidases |
| US6414002B1 (en) | 1999-09-22 | 2002-07-02 | Bristol-Myers Squibb Company | Substituted acid derivatives useful as antidiabetic and antiobesity agents and method |
| US6251391B1 (en) | 1999-10-01 | 2001-06-26 | Klaire Laboratories, Inc. | Compositions containing dipepitidyl peptidase IV and tyrosinase or phenylalaninase for reducing opioid-related symptons |
| US6261794B1 (en) | 1999-10-14 | 2001-07-17 | Saint Louis University | Methods for identifying inhibitors of methionine aminopeptidases |
| US20040152745A1 (en) | 1999-11-12 | 2004-08-05 | Guilford Pharmaceuticals, Inc. | Dipeptidyl peptidase IV inhibitors and methods of making and using dipeptidyl peptidase IV inhibitors |
| AU1916401A (en) | 1999-11-12 | 2001-06-06 | Guilford Pharmaceuticals Inc. | Dipeptidyl peptidase iv inhibitors and methods of making and using dipeptidyl peptidase iv inhibitors |
| GB9928330D0 (en) | 1999-11-30 | 2000-01-26 | Ferring Bv | Novel antidiabetic agents |
| US6380398B2 (en) | 2000-01-04 | 2002-04-30 | Novo Nordisk A/S | Therapeutically active and selective heterocyclic compounds that are inhibitors of the enzyme DPP-IV |
| ES2275654T5 (es) | 2000-01-21 | 2012-06-07 | Novartis Ag | Combinaciones que contienen inhibidores de la dipeptidilpeptidasa-IV y agentes antidiabéticos |
| DE60039194D1 (de) * | 2000-01-24 | 2008-07-24 | Warner Lambert Co | 3-aminochinazolin-2,4-dione als antibakterielle mittel |
| US6569901B2 (en) | 2000-01-28 | 2003-05-27 | Novo Nordisk A/S | Alkynyl-substituted propionic acid derivatives, their preparation and use |
| US7064145B2 (en) | 2000-02-25 | 2006-06-20 | Novo Nordisk A/S | Inhibition of beta cell degeneration |
| US6395767B2 (en) | 2000-03-10 | 2002-05-28 | Bristol-Myers Squibb Company | Cyclopropyl-fused pyrrolidine-based inhibitors of dipeptidyl peptidase IV and method |
| US6608038B2 (en) | 2000-03-15 | 2003-08-19 | Novartis Ag | Methods and compositions for treatment of diabetes and related conditions via gene therapy |
| US6555519B2 (en) | 2000-03-30 | 2003-04-29 | Bristol-Myers Squibb Company | O-glucosylated benzamide SGLT2 inhibitors and method |
| CZ20023234A3 (cs) | 2000-03-31 | 2003-01-15 | Probiodrug Ag | Léčivo proti diabetu |
| US6573096B1 (en) | 2000-04-01 | 2003-06-03 | The Research Foundation At State University Of New York | Compositions and methods for inhibition of cancer invasion and angiogenesis |
| US6545170B2 (en) | 2000-04-13 | 2003-04-08 | Pharmacia Corporation | 2-amino-5, 6 heptenoic acid derivatives useful as nitric oxide synthase inhibitors |
| GB0010183D0 (en) | 2000-04-26 | 2000-06-14 | Ferring Bv | Inhibitors of dipeptidyl peptidase IV |
| GB0010188D0 (en) | 2000-04-26 | 2000-06-14 | Ferring Bv | Inhibitors of dipeptidyl peptidase IV |
| DE10025464A1 (de) | 2000-05-23 | 2001-12-06 | Inst Medizintechnologie Magdeb | Kombinierte Verwendung von Enzyminhibitoren zur Therapie von Autoimmunerkrankungen, bei Transplantationen und Tumorerkrankungen sowie Kombinationen von Enzyminhibitoren umfassende pharmazeutische Zubereitungen |
| AU2001263492A1 (en) | 2000-05-26 | 2001-12-11 | Millennium Pharmaceuticals, Inc. | 21956 and 25856, human aminopeptidases and uses thereof |
| US6783757B2 (en) | 2000-06-01 | 2004-08-31 | Kirkman Group, Inc. | Composition and method for increasing exorphin catabolism to treat autism |
| TW583185B (en) | 2000-06-13 | 2004-04-11 | Novartis Ag | N-(substituted glycyl)-2-cyanopyrrolidines and pharmaceutical composition for inhibiting dipeptidyl peptidase-IV (DPP-IV) or for the prevention or treatment of diseases or conditions associated with elevated levels of DPP-IV comprising the same |
| US6432969B1 (en) | 2000-06-13 | 2002-08-13 | Novartis Ag | N-(substituted glycyl)-2 cyanopyrrolidines, pharmaceutical compositions containing them and their use in inhibiting dipeptidyl peptidase-IV |
| US6627636B2 (en) | 2000-06-15 | 2003-09-30 | Bristol-Myers Squibb Company | HMG-CoA reductase inhibitors and method |
| US6620821B2 (en) | 2000-06-15 | 2003-09-16 | Bristol-Myers Squibb Company | HMG-CoA reductase inhibitors and method |
| GB0014969D0 (en) | 2000-06-19 | 2000-08-09 | Smithkline Beecham Plc | Novel method of treatment |
| US7078397B2 (en) | 2000-06-19 | 2006-07-18 | Smithkline Beecham Corporation | Combinations of dipeptidyl peptidase IV inhibitors and other antidiabetic agents for the treatment of diabetes mellitus |
| MXPA02012272A (es) | 2000-07-04 | 2003-04-25 | Novo Nordisk As | Compuestos heterociclicos que son inhibidores de la enzima dipeptidilpeptidasa-iv. |
| ZA200300255B (en) | 2000-07-20 | 2004-09-28 | Bristol Myers Squibb Pharma Co | Tricyclic 2-pyridone compounds useful as HIV reverse transcriptase inhibitors. |
| WO2002010139A1 (en) | 2000-08-01 | 2002-02-07 | Pharmacia Corporation | Hexahydro-7-1h-azepin-2-yl-haxanoic acid derivatives as inhibitors of inducible nitric oxide synthase |
| JP2004519422A (ja) | 2000-08-04 | 2004-07-02 | ワーナー−ランバート・カンパニー、リミテッド、ライアビリティ、カンパニー | ２−（４−ピリジル）アミノ−６−ジアルコキシフェニルピリド〔２，３−ｄ〕ピリミジン−７−オン |
| CA2418656C (en) | 2000-08-10 | 2011-02-01 | Mitsubishi Pharma Corporation | Proline derivatives and use thereof as drugs |
| US20020165237A1 (en) | 2000-08-11 | 2002-11-07 | Fryburg David Albert | Treatment of the insulin resistance syndrome |
| US20020037829A1 (en) | 2000-08-23 | 2002-03-28 | Aronson Peter S. | Use of DPPIV inhibitors as diuretic and anti-hypertensive agents |
| CN1484709A (zh) | 2000-09-09 | 2004-03-24 | ŦԼ������ѧ�о������ | 分离转移性癌细胞的方法与组合物,及其在检测癌转移性上的应用 |
| AU2001294196B2 (en) | 2000-10-06 | 2005-11-17 | Tanabe Seiyaku Co., Ltd. | Nitrogenous five-membered ring compounds |
| NZ525443A (en) | 2000-10-12 | 2006-04-28 | Ferring Bv | Dipeptidyl peptidase IV related genes |
| AUPR107800A0 (en) | 2000-10-27 | 2000-11-23 | University Of Sydney, The | Peptide and nucleic acid molecule ii |
| US20040043919A1 (en) | 2000-10-27 | 2004-03-04 | Stephan Von Horsten | Method for the treatment of neurological and neuropsychological disorders |
| PT1333887E (pt) | 2000-10-30 | 2006-10-31 | Ortho Mcneil Pharm Inc | Metodo de tratamento de desordens musculares |
| WO2002059343A2 (en) | 2000-10-31 | 2002-08-01 | Vanderbilt University | Biological markers and diagnostic tests for angiotensin converting enzyme inhibitor- and vasopeptidase inhibitor-associated angioedema |
| AU2002225954A1 (en) | 2000-11-08 | 2002-05-21 | The University Of Georgia Research Foundation, Inc. | Dipeptidylpeptidases and methods of use |
| US20030055052A1 (en) | 2000-11-10 | 2003-03-20 | Stefan Peters | FAP-activated anti-tumor compounds |
| US20020155565A1 (en) | 2000-11-10 | 2002-10-24 | Pilar Garin-Chesa | FAP-activated anti-tumor compounds |
| TWI243162B (en) | 2000-11-10 | 2005-11-11 | Taisho Pharmaceutical Co Ltd | Cyanopyrrolidine derivatives |
| US20030203946A1 (en) | 2000-11-17 | 2003-10-30 | Carsten Behrens | Glucagon antagonists/inverse agonists |
| AU2002237664A1 (en) | 2000-11-20 | 2002-05-27 | Bristol-Myers Squibb Company | Pyridone derivatives as AP2 inhibitors |
| KR100883184B1 (ko) | 2000-12-11 | 2009-02-12 | 암젠 인코포레이션 | Ｃｘｃｒ3 길항제 |
| JPWO2002051836A1 (ja) | 2000-12-27 | 2004-04-22 | 協和醗酵工業株式会社 | ジペプチジルペプチダーゼ−ｉｖ阻害剤 |
| DE10100053A1 (de) | 2001-01-02 | 2002-08-22 | Keyneurotek Ag I G | Verwendung von Enzyminhibitoren der Dipeptidylpeptidase IV sowie der Aminopeptidase N und pharmazeutischen Zubereitungen daraus zur Prävention und/oder Therapie Ischämie-bedingter akuter und chronischer neurodegenerativer Prozesse und Erkrankungen |
| WO2002053170A2 (de) | 2001-01-02 | 2002-07-11 | Institut Für Medizintechnologie Magdeburg Gmbh (Imtm) | Kombinierte verwendung von enzyminhibitoren und pharmazeutischen zubereitungen daraus zur therapie und prophylaxe der arteriosklerose, zur therapie und prävention allergischer reaktionen von typ i nach gell und coombs und zur therapie und prävention dermatologischer erkrankungen mit follikulären und epidermalen hyperkeratos |
| GB0101760D0 (en) | 2001-01-23 | 2001-03-07 | Glaxo Group Ltd | Novel protein |
| SK10802003A3 (sk) | 2001-02-02 | 2004-05-04 | Takeda Chemical Industries, Ltd. | Kondenzovaná heterocyklická zlúčenina, jej použitie a jej farmaceutický prípravok |
| TWI255817B (en) | 2001-02-14 | 2006-06-01 | Kissei Pharmaceutical | Glucopyranosyloxybenzylbenzene derivatives and medicinal use thereof |
| MXPA03007349A (es) | 2001-02-24 | 2003-12-04 | Boehringer Ingelheim Pharma | Derivados de xantina, su preparacion y su empleo como medicamentos. |
| US6337069B1 (en) | 2001-02-28 | 2002-01-08 | B.M.R.A. Corporation B.V. | Method of treating rhinitis or sinusitis by intranasally administering a peptidase |
| DE60229922D1 (de) | 2001-03-19 | 2009-01-02 | Novartis Ag | Kombinationen, ein antidiarrhoikum und epothilon oder ein epothilonderivat enthaltend |
| BR0208338A (pt) * | 2001-03-26 | 2004-03-09 | Novartis Ag | Derivados de piridina |
| CA2441092A1 (en) | 2001-03-27 | 2002-10-03 | Merck & Co., Inc. | Dipeptidyl peptidase inhibitors for the treatment or prevention of diabetes |
| FR2822826B1 (fr) | 2001-03-28 | 2003-05-09 | Servier Lab | Nouveaux derives sulfonyles d'alpha-amino-acides, leur procede de preparation et les compositions pharmaceutiques qui les contiennent |
| DE10115921A1 (de) | 2001-03-30 | 2002-10-02 | Boehringer Ingelheim Pharma | Verfahren zur Herstellung von 4,6-Diaminopyrimido[5,4-d]pyrimidinen |
| US6890905B2 (en) | 2001-04-02 | 2005-05-10 | Prosidion Limited | Methods for improving islet signaling in diabetes mellitus and for its prevention |
| GB0109146D0 (en) | 2001-04-11 | 2001-05-30 | Ferring Bv | Treatment of type 2 diabetes |
| PE20021080A1 (es) | 2001-04-12 | 2003-02-12 | Boehringer Ingelheim Int | Un anticuerpo especifico fapo bibh1 en el tratamiento del cancer |
| US6573287B2 (en) | 2001-04-12 | 2003-06-03 | Bristo-Myers Squibb Company | 2,1-oxazoline and 1,2-pyrazoline-based inhibitors of dipeptidyl peptidase IV and method |
| EP1389209B1 (en) | 2001-04-24 | 2009-04-08 | Purdue Research Foundation | Folate mimetics and folate-receptor binding conjugates thereof |
| FR2824825B1 (fr) | 2001-05-15 | 2005-05-06 | Servier Lab | Nouveaux derives d'alpha-amino-acides, leur procede de preparation et les compositions pharmaceutiques qui les contiennent |
| US6825180B2 (en) * | 2001-05-18 | 2004-11-30 | Cell Therapeutics, Inc. | Pyridopyrimidine compounds and their uses |
| US20030060494A1 (en) | 2001-05-18 | 2003-03-27 | Nobuyuki Yasuda | Pharmaceutical use of N-carbamoylazole derivatives |
| US7105556B2 (en) | 2001-05-30 | 2006-09-12 | Bristol-Myers Squibb Company | Conformationally constrained analogs useful as antidiabetic and antiobesity agents and method |
| US6794379B2 (en) | 2001-06-06 | 2004-09-21 | Tularik Inc. | CXCR3 antagonists |
| WO2003000181A2 (en) | 2001-06-20 | 2003-01-03 | Merck & Co., Inc. | Dipeptidyl peptidase inhibitors for the treatment of diabetes |
| DE60224189T2 (de) | 2001-06-20 | 2008-12-11 | Merck & Co., Inc. | Dipeptidylpeptidase-hemmer zur behandlung von diabetes |
| US7196201B2 (en) | 2001-06-27 | 2007-03-27 | Smithkline Beecham Corporation | Pyrrolidines as dipeptidyl peptidase inhibitors |
| US7183290B2 (en) | 2001-06-27 | 2007-02-27 | Smithkline Beecham Corporation | Fluoropyrrolidines as dipeptidyl peptidase inhibitors |
| US7368421B2 (en) | 2001-06-27 | 2008-05-06 | Probiodrug Ag | Use of dipeptidyl peptidase IV inhibitors in the treatment of multiple sclerosis |
| DE10154689A1 (de) | 2001-11-09 | 2003-05-22 | Probiodrug Ag | Substituierte Aminoketonverbindungen |
| CA2419888A1 (en) | 2001-06-27 | 2003-01-09 | Probiodrug Ag | Peptide structures useful for competitive modulation of dipeptidyl peptidase iv catalysis |
| ES2296979T3 (es) | 2001-06-27 | 2008-05-01 | Smithkline Beecham Corporation | Fluoropirrolidinas como inhibidores de dipeptidil peptidasa. |
| US20030130199A1 (en) | 2001-06-27 | 2003-07-10 | Von Hoersten Stephan | Dipeptidyl peptidase IV inhibitors and their uses as anti-cancer agents |
| US20030135023A1 (en) | 2001-06-27 | 2003-07-17 | Hans-Ulrich Demuth | Peptide structures useful for competitive modulation of dipeptidyl peptidase IV catalysis |
| CA2418543A1 (en) | 2001-06-27 | 2003-01-09 | Probiodrug Ag | New dipeptidyl peptidase iv inhibitors and their uses as anti-cancer agents |
| DE10150203A1 (de) | 2001-10-12 | 2003-04-17 | Probiodrug Ag | Peptidylketone als Inhibitoren der DPIV |
| US6869947B2 (en) | 2001-07-03 | 2005-03-22 | Novo Nordisk A/S | Heterocyclic compounds that are inhibitors of the enzyme DPP-IV |
| UA74912C2 (en) | 2001-07-06 | 2006-02-15 | Merck & Co Inc | Beta-aminotetrahydroimidazo-(1,2-a)-pyrazines and tetratriazolo-(4,3-a)-pyrazines as inhibitors of dipeptylpeptidase for the treatment or prevention of diabetes |
| US20030144350A1 (en) | 2001-07-20 | 2003-07-31 | Adipogenix, Inc. | Fat accumulation-modulation compounds |
| EP1417220A2 (en) | 2001-08-13 | 2004-05-12 | Probiodrug AG | Irreversible cysteine protease inhibitors of legumain |
| US9048965B2 (en) | 2001-08-24 | 2015-06-02 | Mark Henrik Sandstrom | Input-controllable dynamic cross-connect |
| DE10143840A1 (de) | 2001-09-06 | 2003-03-27 | Probiodrug Ag | Neue Inhibitoren der Dipeptidylpeptidase I |
| US6844316B2 (en) | 2001-09-06 | 2005-01-18 | Probiodrug Ag | Inhibitors of dipeptidyl peptidase I |
| TWI246510B (en) | 2001-09-14 | 2006-01-01 | Mitsubishi Pharma Corp | Thiazolidine derivatives and pharmaceutical uses thereof |
| US6673829B2 (en) | 2001-09-14 | 2004-01-06 | Novo Nordisk A/S | Aminoazetidine,-pyrrolidine and -piperidine derivatives |
| US20030186963A1 (en) | 2001-09-14 | 2003-10-02 | Dorwald Florencio Zaragoza | Substituted piperidines |
| WO2003024965A2 (en) | 2001-09-19 | 2003-03-27 | Novo Nordisk A/S | Heterocyclic compounds that are inhibitors of the enzyme dpp-iv |
| ES2329881T3 (es) | 2001-09-21 | 2009-12-02 | Bristol-Myers Squibb Company | Compuestos que contienen lactama y derivados de los mismos como inhibidores del factor xa. |
| US7019010B2 (en) | 2001-09-27 | 2006-03-28 | Novertis Ag | Combinations |
| NZ531870A (en) | 2001-10-01 | 2005-08-26 | Bristol Myers Squibb Co | Spiro-hydantoin compounds useful as anti-inflammatory agents |
| WO2003030946A1 (en) | 2001-10-09 | 2003-04-17 | Novartis Ag | Regulation of insulin production |
| US7064135B2 (en) | 2001-10-12 | 2006-06-20 | Novo Nordisk Inc. | Substituted piperidines |
| GB0125445D0 (en) | 2001-10-23 | 2001-12-12 | Ferring Bv | Protease Inhibitors |
| US6861440B2 (en) | 2001-10-26 | 2005-03-01 | Hoffmann-La Roche Inc. | DPP IV inhibitors |
| EP1442028A4 (en) | 2001-11-06 | 2009-11-04 | Bristol Myers Squibb Co | SUBSTITUTED ACID DERIVATIVES, WHICH APPRECIATE AS ANTIDIBILICS AND AGENTS AGAINST OBESITAS, AND METHODS |
| US20030125304A1 (en) | 2001-11-09 | 2003-07-03 | Hans-Ulrich Demuth | Substituted amino ketone compounds |
| JP2005511636A (ja) | 2001-11-26 | 2005-04-28 | トラスティーズ オブ タフツ カレッジ | 自己免疫疾患の治療方法及びそれに関する試薬 |
| AU2002357767C1 (en) | 2001-11-26 | 2009-03-19 | Trustees Of Tufts College | Peptidomimetic inhibitors of post-proline cleaving enzymes |
| AU2002350217A1 (en) | 2001-12-04 | 2003-06-17 | Bristol-Myers Squibb Company | Glycinamides as factor xa inhibitors |
| JP2005518376A (ja) | 2001-12-14 | 2005-06-23 | ノボ ノルディスク アクティーゼルスカブ | 化合物およびホルモン感受性リパーゼの活性を低下させるためのその使用 |
| TW200301698A (en) | 2001-12-21 | 2003-07-16 | Bristol Myers Squibb Co | Acridone inhibitors of IMPDH enzyme |
| US20030171411A1 (en) | 2001-12-21 | 2003-09-11 | Kodra Janos Tibor | Amide derivatives as therapeutic agents |
| US6727261B2 (en) | 2001-12-27 | 2004-04-27 | Hoffman-La Roche Inc. | Pyrido[2,1-A]Isoquinoline derivatives |
| ES2280596T3 (es) | 2001-12-29 | 2007-09-16 | Novo Nordisk A/S | Uso combinado de un compuesto de glp-1 y un inhibidor de una aldosa reductasa. |
| AU2003201274A1 (en) | 2002-01-11 | 2003-07-24 | Novo Nordisk A/S | Compositions comprising inhibitors of dpp-iv and nep enzymes for the treatment of diabetes |
| AU2003218969A1 (en) | 2002-02-01 | 2003-09-02 | Probiodrug Ag | Modulation of t lymphocytes using dp iv inhibitors |
| US7101898B2 (en) | 2002-02-01 | 2006-09-05 | Novo Nordisk A/S | Amides of aminoalkyl-substituted azetidines, pyrrolidines, piperidines and azepanes |
| KR100608414B1 (ko) | 2002-02-13 | 2006-08-02 | 에프. 호프만-라 로슈 아게 | 신규한 피리딘- 및 피리미딘-유도체 |
| EP1476429B1 (en) | 2002-02-13 | 2005-11-16 | F. Hoffmann-La Roche Ag | Novel pyridine- and quinoline-derivatives |
| HRP20040716A2 (en) | 2002-02-27 | 2005-02-28 | Pfizer Products Inc. | Acc inhibitors |
| DE60217186T2 (de) | 2002-02-28 | 2007-09-27 | Prosidion Ltd. | Dpiv-inhibitoren auf glutaminbasis |
| AU2003228283A1 (en) | 2002-03-07 | 2003-09-22 | X-Ceptor Therapeutics, Inc. | Quinazolinone modulators of nuclear receptors |
| US6947847B2 (en) | 2002-03-08 | 2005-09-20 | Wisconsin Alumni Research Foundation | Method to design therapeutically important compounds |
| US20030232761A1 (en) | 2002-03-28 | 2003-12-18 | Hinke Simon A. | Novel analogues of glucose-dependent insulinotropic polypeptide |
| US20040106802A1 (en) | 2002-04-08 | 2004-06-03 | Torrent Pharmaceuticals Ltd. | Novel compounds and therapeutic uses thereof |
| RU2004132719A (ru) | 2002-04-08 | 2005-08-27 | Торрент Фармасьютикалз Лтд. (In) | Тиазолидин-4-карбонитрилы и их аналоги, применение указанных соединений в качестве ингибиторов дипептидилпептидаз |
| EP2204181A3 (en) | 2002-04-30 | 2010-09-22 | Trustees Of Tufts College | Protease inhibitors |
| TW200307667A (en) | 2002-05-06 | 2003-12-16 | Bristol Myers Squibb Co | Sulfonylaminovalerolactams and derivatives thereof as factor Xa inhibitors |
| US7057046B2 (en) | 2002-05-20 | 2006-06-06 | Bristol-Myers Squibb Company | Lactam glycogen phosphorylase inhibitors and method of use |
| DE60333937D1 (de) | 2002-05-23 | 2010-10-07 | Novartis Vaccines & Diagnostic | Substituierte quinazolinone verbindungen |
| GB0212412D0 (en) | 2002-05-29 | 2002-07-10 | Novartis Ag | Combination of organic compounds |
| US6710040B1 (en) | 2002-06-04 | 2004-03-23 | Pfizer Inc. | Fluorinated cyclic amides as dipeptidyl peptidase IV inhibitors |
| WO2003101449A2 (en) | 2002-06-04 | 2003-12-11 | Pfizer Products Inc. | Process for the preparation of 3,3,4,4-tetrafluoropyrrolidine and derivatives thereof |
| CA2485641C (en) | 2002-06-06 | 2010-12-14 | Eisai Co., Ltd. | Novel condensed imidazole derivatives |
| AU2003276648A1 (en) | 2002-06-17 | 2003-12-31 | Bristol-Myers Squibb Company | Benzodiazepine inhibitors of mitochondial f¿1?f¿0? atp hydrolase and methods of inhibiting f¿1?f¿0? atp hydrolase |
| US20040054171A1 (en) | 2002-07-04 | 2004-03-18 | Jensen Anette Frost | Polymorphic forms of a 4H-thieno[3,2-E]-1,2,4-thiadiazine 1,1-dioxide derivative |
| AU2003246972A1 (en) | 2002-08-06 | 2004-02-23 | Astrazeneca Ab | Condensed pyridines and pyrimidines with tie2 (tek) activity |
| AU2002331226A1 (en) | 2002-08-09 | 2004-03-11 | Prosidion Ltd. | Methods for improving islet signaling in diabetes mellitus and for its prevention |
| US7407955B2 (en) | 2002-08-21 | 2008-08-05 | Boehringer Ingelheim Pharma Gmbh & Co., Kg | 8-[3-amino-piperidin-1-yl]-xanthines, the preparation thereof and their use as pharmaceutical compositions |
| US7495005B2 (en) | 2002-08-22 | 2009-02-24 | Boehringer Ingelheim Pharma Gmbh & Co. Kg | Xanthine derivatives, their preparation and their use in pharmaceutical compositions |
| DE10238470A1 (de) * | 2002-08-22 | 2004-03-04 | Boehringer Ingelheim Pharma Gmbh & Co. Kg | Neue Xanthinderivate, deren Herstellung und deren Verwendung als Arzneimittel |
| US7569574B2 (en) | 2002-08-22 | 2009-08-04 | Boehringer Ingelheim Pharma Gmbh & Co. Kg | Purine derivatives, the preparation thereof and their use as pharmaceutical compositions |
| US20040058876A1 (en) | 2002-09-18 | 2004-03-25 | Torsten Hoffmann | Secondary binding site of dipeptidyl peptidase IV (DP IV) |
| AU2003293311A1 (en) | 2002-09-18 | 2004-04-23 | Prosidion Ltd. | Secondary binding site of dipeptidyl peptidase iv (dp iv) |
| US7262207B2 (en) | 2002-09-19 | 2007-08-28 | Abbott Laboratories | Pharmaceutical compositions as inhibitors of dipeptidyl peptidase-IV (DPP-IV) |
| US6869966B2 (en) | 2002-09-30 | 2005-03-22 | Banyu Pharmaceutical Co., Ltd. | N-substituted-2-oxodihydropyridine derivatives |
| PL216527B1 (pl) | 2002-10-18 | 2014-04-30 | Merck & Co Inc | Związki ß-aminoheterocykliczne i kompozycja farmaceutyczna |
| AU2003301662A1 (en) | 2002-10-21 | 2004-05-13 | Bristol-Myers Squibb Company | Quinazolinones and derivatives thereof as factor xa inhibitors |
| US6995180B2 (en) | 2002-10-23 | 2006-02-07 | Bristol Myers Squibb Company | Glycinenitrile-based inhibitors of dipeptidyl peptidase IV and methods |
| US7482337B2 (en) | 2002-11-08 | 2009-01-27 | Boehringer Ingelheim Pharma Gmbh & Co. Kg | Xanthine derivatives, the preparation thereof and their use as pharmaceutical compositions |
| WO2004046106A1 (en) | 2002-11-18 | 2004-06-03 | Pfizer Products Inc. | Dipeptidyl peptidase iv inhibiting fluorinated cyclic amides |
| DE10254304A1 (de) | 2002-11-21 | 2004-06-03 | Boehringer Ingelheim Pharma Gmbh & Co. Kg | Neue Xanthinderivate, deren Herstellung und deren Verwendung als Arzneimittel |
| UY28103A1 (es) * | 2002-12-03 | 2004-06-30 | Boehringer Ingelheim Pharma | Nuevas imidazo-piridinonas sustituidas, su preparación y su empleo como medicacmentos |
| US7109192B2 (en) | 2002-12-03 | 2006-09-19 | Boehringer Ingelheim Pharma Gmbh & Co Kg | Substituted imidazo-pyridinones and imidazo-pyridazinones, the preparation thereof and their use as pharmaceutical compositions |
| CL2004000234A1 (es) | 2003-02-12 | 2005-04-15 | Biogen Idec Inc | Compuestos derivados 3-(piridin-2-il)-4-heteroaril-pirazol sustituidos, antagonistas de aik5 y/o aik4; composicion farmaceutica y uso del compuesto en el tratamiento de desordenes fibroticos como esclerodermia, lupus nefritico, cicatrizacion de herid |
| US7148246B2 (en) | 2003-02-27 | 2006-12-12 | Sanofi-Aventis Deutschland Gmbh | Cycloalkyl derivatives having bioisosteric carboxylic acid groups, processes for their preparation and their use as pharmaceuticals |
| US20050014732A1 (en) | 2003-03-14 | 2005-01-20 | Pharmacia Corporation | Combination of an aldosterone receptor antagonist and an anti-diabetic agent |
| KR20050122220A (ko) | 2003-03-25 | 2005-12-28 | 다케다 샌디에고, 인코포레이티드 | 디펩티딜 펩티다제 억제제 |
| WO2004099134A2 (en) | 2003-05-05 | 2004-11-18 | Prosidion Ltd. | Glutaminyl based dp iv-inhibitors |
| US7381537B2 (en) | 2003-05-05 | 2008-06-03 | Probiodrug Ag | Use of inhibitors of glutaminyl cyclases for treatment and prevention of disease |
| EP1625122A1 (en) | 2003-05-14 | 2006-02-15 | Takeda San Diego, Inc. | Dipeptidyl peptidase inhibitors |
| US7566707B2 (en) | 2003-06-18 | 2009-07-28 | Boehringer Ingelheim International Gmbh | Imidazopyridazinone and imidazopyridone derivatives, the preparation thereof and their use as pharmaceutical compositions |
| DK1638970T3 (da) | 2003-06-20 | 2011-01-03 | Hoffmann La Roche | Pyrid (2, 1-A)-isoquinolinderivater som DPP-IV-inhibitorer |
| AU2004251829B2 (en) | 2003-06-20 | 2009-12-17 | F. Hoffmann-La Roche Ag | Hexahydropyridoisoqinolines as DPP-IV inhibitors |
| JO2625B1 (en) | 2003-06-24 | 2011-11-01 | ميرك شارب اند دوم كوربوريشن | Phosphoric acid salts of dipeptidyl betidase inhibitor 4 |
| US6995183B2 (en) | 2003-08-01 | 2006-02-07 | Bristol Myers Squibb Company | Adamantylglycine-based inhibitors of dipeptidyl peptidase IV and methods |
| WO2005019168A2 (en) | 2003-08-20 | 2005-03-03 | Pfizer Products Inc. | Fluorinated lysine derivatives as dipeptidyl peptidase iv inhibitors |
-
2005
- 2005-07-14 WO PCT/US2005/025070 patent/WO2006019965A2/en not_active Ceased
- 2005-07-15 US US11/183,335 patent/US7825242B2/en not_active Expired - Fee Related
- 2005-07-15 JP JP2007521673A patent/JP4945443B2/ja not_active Expired - Fee Related
- 2005-07-15 EP EP05772260A patent/EP1773832A2/en not_active Withdrawn
- 2005-07-15 WO PCT/US2005/025153 patent/WO2006020017A2/en not_active Ceased
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