NO332232B1 - Dipeptidylpeptidaseinhibitorer og farmasoytisk sammensetning inneholdende disse - Google Patents

Info

Publication number

NO332232B1

NO332232B1 NO20064669A NO20064669A NO332232B1 NO 332232 B1 NO332232 B1 NO 332232B1 NO 20064669 A NO20064669 A NO 20064669A NO 20064669 A NO20064669 A NO 20064669A NO 332232 B1 NO332232 B1 NO 332232B1

Authority

NO

Norway

Prior art keywords

alkyl

phenyl

group

amino

dpp

Prior art date

2004-03-15

Links

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• 239000008194 pharmaceutical composition Substances 0.000 title claims description 4
• 102000003779 Dipeptidyl-peptidases and tripeptidyl-peptidases Human genes 0.000 title description 4
• 108090000194 Dipeptidyl-peptidases and tripeptidyl-peptidases Proteins 0.000 title description 4
• 239000000137 peptide hydrolase inhibitor Substances 0.000 title 1
• 150000001875 compounds Chemical class 0.000 claims abstract description 288
• 125000000217 alkyl group Chemical group 0.000 claims description 343
• -1 3-amino-piperidinyl-1-yl Chemical group 0.000 claims description 295
• 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims description 259
• 125000000753 cycloalkyl group Chemical group 0.000 claims description 164
• 125000000008 (C1-C10) alkyl group Chemical group 0.000 claims description 116
• 239000000203 mixture Substances 0.000 claims description 80
• 150000003839 salts Chemical class 0.000 claims description 56
• 125000001475 halogen functional group Chemical group 0.000 claims description 16
• 239000004480 active ingredient Substances 0.000 claims description 6
• 125000004194 piperazin-1-yl group Chemical group [H]N1C([H])([H])C([H])([H])N(*)C([H])([H])C1([H])[H] 0.000 claims description 5
• ODPLRMYULKQCHO-LJQANCHMSA-N 2-[[6-[(3r)-3-amino-3-methylpiperidin-1-yl]-3-methyl-2,4-dioxopyrimidin-1-yl]methyl]-4-fluorobenzonitrile Chemical compound C=1C(F)=CC=C(C#N)C=1CN1C(=O)N(C)C(=O)C=C1N1CCC[C@@](C)(N)C1 ODPLRMYULKQCHO-LJQANCHMSA-N 0.000 claims description 4
• IWYJYHUNXVAVAA-OAHLLOKOSA-N trelagliptin Chemical compound C=1C(F)=CC=C(C#N)C=1CN1C(=O)N(C)C(=O)C=C1N1CCC[C@@H](N)C1 IWYJYHUNXVAVAA-OAHLLOKOSA-N 0.000 claims description 4
• GZBXRROZKDWTHE-UHFFFAOYSA-N 6-(3-aminopiperidin-1-yl)-1-[(2-bromo-5-fluorophenyl)methyl]-3-methylpyrimidine-2,4-dione Chemical compound C=1C(F)=CC=C(Br)C=1CN1C(=O)N(C)C(=O)C=C1N1CCCC(N)C1 GZBXRROZKDWTHE-UHFFFAOYSA-N 0.000 claims description 3
• ZOZBXLMDTJHPKM-UHFFFAOYSA-N 6-(3-aminopiperidin-1-yl)-1-[(2-bromophenyl)methyl]-3-methylpyrimidine-2,4-dione Chemical compound C=1C=CC=C(Br)C=1CN1C(=O)N(C)C(=O)C=C1N1CCCC(N)C1 ZOZBXLMDTJHPKM-UHFFFAOYSA-N 0.000 claims description 3
• GZBQHUMIMKAYHA-UHFFFAOYSA-N 6-(3-aminopiperidin-1-yl)-1-[(2-chloro-5-fluorophenyl)methyl]-3-methylpyrimidine-2,4-dione Chemical compound C=1C(F)=CC=C(Cl)C=1CN1C(=O)N(C)C(=O)C=C1N1CCCC(N)C1 GZBQHUMIMKAYHA-UHFFFAOYSA-N 0.000 claims description 3
• NOKFOTRWCQJAKB-UHFFFAOYSA-N 2-[[6-(3-aminopiperidin-1-yl)-3-ethyl-2,4-dioxopyrimidin-1-yl]methyl]benzonitrile Chemical compound C=1C=CC=C(C#N)C=1CN1C(=O)N(CC)C(=O)C=C1N1CCCC(N)C1 NOKFOTRWCQJAKB-UHFFFAOYSA-N 0.000 claims description 2
• SIOPCTQIGVRHCI-CYBMUJFWSA-N 6-[(3r)-3-aminopiperidin-1-yl]-1-[(2,5-dichlorophenyl)methyl]-3-methylpyrimidine-2,4-dione Chemical compound C=1C(Cl)=CC=C(Cl)C=1CN1C(=O)N(C)C(=O)C=C1N1CCC[C@@H](N)C1 SIOPCTQIGVRHCI-CYBMUJFWSA-N 0.000 claims 1
• 102100025012 Dipeptidyl peptidase 4 Human genes 0.000 abstract description 181
• 108010067722 Dipeptidyl Peptidase 4 Proteins 0.000 abstract description 168
• 238000000034 method Methods 0.000 abstract description 66
• 102000035195 Peptidases Human genes 0.000 abstract description 10
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• 239000004365 Protease Substances 0.000 abstract description 9
• 229910002091 carbon monoxide Inorganic materials 0.000 abstract description 9
• 239000003814 drug Substances 0.000 abstract description 6
• 125000002915 carbonyl group Chemical group [*:2]C([*:1])=O 0.000 description 130
• 125000001072 heteroaryl group Chemical group 0.000 description 130
• 125000003118 aryl group Chemical group 0.000 description 124
• 125000000475 sulfinyl group Chemical group [*:2]S([*:1])=O 0.000 description 119
• 125000005842 heteroatom Chemical group 0.000 description 110
• 125000000472 sulfonyl group Chemical group *S(*)(=O)=O 0.000 description 102
• 125000001841 imino group Chemical group [H]N=* 0.000 description 98
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• 125000002924 primary amino group Chemical group [H]N([H])* 0.000 description 63
• 125000000592 heterocycloalkyl group Chemical group 0.000 description 59
• 239000001257 hydrogen Substances 0.000 description 58
• 229910052739 hydrogen Inorganic materials 0.000 description 58
• 125000002813 thiocarbonyl group Chemical group *C(*)=S 0.000 description 58
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• UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 description 41
• 125000005843 halogen group Chemical group 0.000 description 40
• 239000000243 solution Substances 0.000 description 40
• IAZDPXIOMUYVGZ-UHFFFAOYSA-N Dimethylsulphoxide Chemical compound CS(C)=O IAZDPXIOMUYVGZ-UHFFFAOYSA-N 0.000 description 33
• 125000004429 atom Chemical group 0.000 description 32
• 238000011282 treatment Methods 0.000 description 32
• 125000004093 cyano group Chemical group *C#N 0.000 description 31
• 125000004432 carbon atom Chemical group C* 0.000 description 30
• 125000001424 substituent group Chemical group 0.000 description 30
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• 239000003795 chemical substances by application Substances 0.000 description 24
• QJGQUHMNIGDVPM-UHFFFAOYSA-N nitrogen group Chemical group [N] QJGQUHMNIGDVPM-UHFFFAOYSA-N 0.000 description 24
• ZMXDDKWLCZADIW-UHFFFAOYSA-N N,N-Dimethylformamide Chemical compound CN(C)C=O ZMXDDKWLCZADIW-UHFFFAOYSA-N 0.000 description 23
• 125000004390 alkyl sulfonyl group Chemical group 0.000 description 23
• 125000004397 aminosulfonyl group Chemical group NS(=O)(=O)* 0.000 description 23
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• 125000005143 heteroarylsulfonyl group Chemical group 0.000 description 23
• 125000004435 hydrogen atom Chemical group [H]* 0.000 description 23
• YMWUJEATGCHHMB-UHFFFAOYSA-N Dichloromethane Chemical compound ClCCl YMWUJEATGCHHMB-UHFFFAOYSA-N 0.000 description 21
• OKKJLVBELUTLKV-UHFFFAOYSA-N Methanol Chemical compound OC OKKJLVBELUTLKV-UHFFFAOYSA-N 0.000 description 21
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• PEDCQBHIVMGVHV-UHFFFAOYSA-N Glycerine Chemical compound OCC(O)CO PEDCQBHIVMGVHV-UHFFFAOYSA-N 0.000 description 19
• 239000002904 solvent Substances 0.000 description 19
• 239000002585 base Substances 0.000 description 18
• JFDZBHWFFUWGJE-UHFFFAOYSA-N benzonitrile Substances N#CC1=CC=CC=C1 JFDZBHWFFUWGJE-UHFFFAOYSA-N 0.000 description 18
• WYURNTSHIVDZCO-UHFFFAOYSA-N Tetrahydrofuran Chemical compound C1CCOC1 WYURNTSHIVDZCO-UHFFFAOYSA-N 0.000 description 17
• 230000002401 inhibitory effect Effects 0.000 description 17
• 125000004433 nitrogen atom Chemical group N* 0.000 description 17
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• 125000000325 methylidene group Chemical group [H]C([H])=* 0.000 description 16
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• HEMHJVSKTPXQMS-UHFFFAOYSA-M Sodium hydroxide Chemical compound [OH-].[Na+] HEMHJVSKTPXQMS-UHFFFAOYSA-M 0.000 description 15
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• HBAQYPYDRFILMT-UHFFFAOYSA-N 8-[3-(1-cyclopropylpyrazol-4-yl)-1H-pyrazolo[4,3-d]pyrimidin-5-yl]-3-methyl-3,8-diazabicyclo[3.2.1]octan-2-one Chemical class C1(CC1)N1N=CC(=C1)C1=NNC2=C1N=C(N=C2)N1C2C(N(CC1CC2)C)=O HBAQYPYDRFILMT-UHFFFAOYSA-N 0.000 description 12
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• RAXXELZNTBOGNW-UHFFFAOYSA-N imidazole Natural products C1=CNC=N1 RAXXELZNTBOGNW-UHFFFAOYSA-N 0.000 description 12
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• 101000930822 Giardia intestinalis Dipeptidyl-peptidase 4 Proteins 0.000 description 10
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