HRP20161011T1 - Aril dihidropiridinoni i piperidinoni kao inhibitori mgat2 - Google Patents
Aril dihidropiridinoni i piperidinoni kao inhibitori mgat2 Download PDFInfo
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- HRP20161011T1 HRP20161011T1 HRP20161011TT HRP20161011T HRP20161011T1 HR P20161011 T1 HRP20161011 T1 HR P20161011T1 HR P20161011T T HRP20161011T T HR P20161011TT HR P20161011 T HRP20161011 T HR P20161011T HR P20161011 T1 HRP20161011 T1 HR P20161011T1
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- 239000003112 inhibitor Substances 0.000 title claims 2
- 125000003118 aryl group Chemical group 0.000 title 1
- XUWHAWMETYGRKB-UHFFFAOYSA-N piperidin-2-one Chemical class O=C1CCCCN1 XUWHAWMETYGRKB-UHFFFAOYSA-N 0.000 title 1
- 150000001875 compounds Chemical class 0.000 claims 52
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 claims 25
- 125000000217 alkyl group Chemical group 0.000 claims 21
- 125000005843 halogen group Chemical group 0.000 claims 19
- -1 -CONH(CH2)1-8 Ph Chemical group 0.000 claims 17
- 150000003839 salts Chemical class 0.000 claims 17
- 125000004432 carbon atom Chemical group C* 0.000 claims 16
- 229910052739 hydrogen Inorganic materials 0.000 claims 15
- 125000004765 (C1-C4) haloalkyl group Chemical group 0.000 claims 12
- 229910052799 carbon Inorganic materials 0.000 claims 10
- 125000000229 (C1-C4)alkoxy group Chemical group 0.000 claims 9
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 claims 9
- 125000003545 alkoxy group Chemical group 0.000 claims 9
- 239000003795 chemical substances by application Substances 0.000 claims 9
- 229910052731 fluorine Inorganic materials 0.000 claims 9
- 125000004767 (C1-C4) haloalkoxy group Chemical group 0.000 claims 8
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 claims 7
- 125000004008 6 membered carbocyclic group Chemical group 0.000 claims 7
- 125000001072 heteroaryl group Chemical group 0.000 claims 7
- 125000005842 heteroatom Chemical group 0.000 claims 7
- 229910052760 oxygen Inorganic materials 0.000 claims 7
- 229910052717 sulfur Inorganic materials 0.000 claims 7
- 125000000623 heterocyclic group Chemical group 0.000 claims 6
- 239000012453 solvate Substances 0.000 claims 6
- 229910052801 chlorine Inorganic materials 0.000 claims 5
- 239000003814 drug Substances 0.000 claims 5
- 125000004076 pyridyl group Chemical group 0.000 claims 5
- 229940124597 therapeutic agent Drugs 0.000 claims 5
- 125000006645 (C3-C4) cycloalkyl group Chemical group 0.000 claims 4
- 229910052757 nitrogen Inorganic materials 0.000 claims 4
- 208000008338 non-alcoholic fatty liver disease Diseases 0.000 claims 4
- 125000002971 oxazolyl group Chemical group 0.000 claims 4
- 125000003226 pyrazolyl group Chemical group 0.000 claims 4
- 125000003831 tetrazolyl group Chemical group 0.000 claims 4
- 125000006569 (C5-C6) heterocyclic group Chemical group 0.000 claims 3
- 125000000392 cycloalkenyl group Chemical group 0.000 claims 3
- 125000001511 cyclopentyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])(*)C1([H])[H] 0.000 claims 3
- 125000001559 cyclopropyl group Chemical group [H]C1([H])C([H])([H])C1([H])* 0.000 claims 3
- 125000004438 haloalkoxy group Chemical group 0.000 claims 3
- 125000001188 haloalkyl group Chemical group 0.000 claims 3
- 125000001183 hydrocarbyl group Chemical group 0.000 claims 3
- 125000002757 morpholinyl group Chemical group 0.000 claims 3
- 239000008194 pharmaceutical composition Substances 0.000 claims 3
- 125000004307 pyrazin-2-yl group Chemical group [H]C1=C([H])N=C(*)C([H])=N1 0.000 claims 3
- 125000003373 pyrazinyl group Chemical group 0.000 claims 3
- 125000004191 (C1-C6) alkoxy group Chemical group 0.000 claims 2
- 125000000171 (C1-C6) haloalkyl group Chemical group 0.000 claims 2
- 125000004209 (C1-C8) alkyl group Chemical group 0.000 claims 2
- 125000006648 (C1-C8) haloalkyl group Chemical group 0.000 claims 2
- 125000004182 2-chlorophenyl group Chemical group [H]C1=C([H])C(Cl)=C(*)C([H])=C1[H] 0.000 claims 2
- 208000032928 Dyslipidaemia Diseases 0.000 claims 2
- 102000015779 HDL Lipoproteins Human genes 0.000 claims 2
- 108010010234 HDL Lipoproteins Proteins 0.000 claims 2
- 102000007330 LDL Lipoproteins Human genes 0.000 claims 2
- 108010007622 LDL Lipoproteins Proteins 0.000 claims 2
- 208000017170 Lipid metabolism disease Diseases 0.000 claims 2
- JCXJVPUVTGWSNB-UHFFFAOYSA-N Nitrogen dioxide Chemical compound O=[N]=O JCXJVPUVTGWSNB-UHFFFAOYSA-N 0.000 claims 2
- 239000003472 antidiabetic agent Substances 0.000 claims 2
- 239000003524 antilipemic agent Substances 0.000 claims 2
- 239000002830 appetite depressant Substances 0.000 claims 2
- 125000006367 bivalent amino carbonyl group Chemical group [H]N([*:1])C([*:2])=O 0.000 claims 2
- 235000019256 formaldehyde Nutrition 0.000 claims 2
- 239000001257 hydrogen Substances 0.000 claims 2
- 125000004435 hydrogen atom Chemical class [H]* 0.000 claims 2
- 125000002962 imidazol-1-yl group Chemical group [*]N1C([H])=NC([H])=C1[H] 0.000 claims 2
- 125000002883 imidazolyl group Chemical group 0.000 claims 2
- 125000000842 isoxazolyl group Chemical group 0.000 claims 2
- 239000000203 mixture Substances 0.000 claims 2
- 208000031225 myocardial ischemia Diseases 0.000 claims 2
- 206010053219 non-alcoholic steatohepatitis Diseases 0.000 claims 2
- 125000001715 oxadiazolyl group Chemical group 0.000 claims 2
- 125000004430 oxygen atom Chemical group O* 0.000 claims 2
- 125000001037 p-tolyl group Chemical group [H]C1=C([H])C(=C([H])C([H])=C1*)C([H])([H])[H] 0.000 claims 2
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 2
- 125000001424 substituent group Chemical group 0.000 claims 2
- 125000000335 thiazolyl group Chemical group 0.000 claims 2
- 125000001425 triazolyl group Chemical group 0.000 claims 2
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 claims 2
- AEMPUAWUDAMJBV-JOCHJYFZSA-N (2r)-4-(4-methylphenyl)-5-(2h-tetrazol-5-yl)-2-[4-(4,4,4-trifluorobutoxy)phenyl]-2-(trifluoromethyl)-1,3-dihydropyridin-6-one Chemical compound C1=CC(C)=CC=C1C(C[C@@](NC1=O)(C=2C=CC(OCCCC(F)(F)F)=CC=2)C(F)(F)F)=C1C1=NN=NN1 AEMPUAWUDAMJBV-JOCHJYFZSA-N 0.000 claims 1
- FBBPRPJENPWDPL-GDLZYMKVSA-N (2r)-n-(4-methoxyphenyl)-4-(4-methylphenyl)-6-oxo-2-[4-(4,4,4-trifluorobutoxy)phenyl]-2-(trifluoromethyl)-1,3-dihydropyridine-5-carboxamide Chemical compound C1=CC(OC)=CC=C1NC(=O)C1=C(C=2C=CC(C)=CC=2)C[C@](C(F)(F)F)(C=2C=CC(OCCCC(F)(F)F)=CC=2)NC1=O FBBPRPJENPWDPL-GDLZYMKVSA-N 0.000 claims 1
- AEMPUAWUDAMJBV-QFIPXVFZSA-N (2s)-4-(4-methylphenyl)-5-(2h-tetrazol-5-yl)-2-[4-(4,4,4-trifluorobutoxy)phenyl]-2-(trifluoromethyl)-1,3-dihydropyridin-6-one Chemical compound C1=CC(C)=CC=C1C(C[C@](NC1=O)(C=2C=CC(OCCCC(F)(F)F)=CC=2)C(F)(F)F)=C1C1=NN=NN1 AEMPUAWUDAMJBV-QFIPXVFZSA-N 0.000 claims 1
- WDLHNOKAVCEXRE-DEOSSOPVSA-N (2s)-4-(4-methylphenyl)-5-(2h-tetrazol-5-yl)-2-[4-(6,6,6-trifluorohexoxy)phenyl]-2-(trifluoromethyl)-1,3-dihydropyridin-6-one Chemical compound C1=CC(C)=CC=C1C(C[C@](NC1=O)(C=2C=CC(OCCCCCC(F)(F)F)=CC=2)C(F)(F)F)=C1C1=NNN=N1 WDLHNOKAVCEXRE-DEOSSOPVSA-N 0.000 claims 1
- VFSDYCUMBLVRMP-MHZLTWQESA-N (2s)-4-(4-methylphenyl)-5-phenoxy-2-[4-(4,4,4-trifluorobutoxy)phenyl]-2-(trifluoromethyl)-1,3-dihydropyridin-6-one Chemical compound C1=CC(C)=CC=C1C(C[C@](NC1=O)(C=2C=CC(OCCCC(F)(F)F)=CC=2)C(F)(F)F)=C1OC1=CC=CC=C1 VFSDYCUMBLVRMP-MHZLTWQESA-N 0.000 claims 1
- KTEKFLCACKLBMQ-NRFANRHFSA-N (2s)-5-amino-4-(4-methylphenyl)-2-[4-(4,4,4-trifluorobutoxy)phenyl]-2-(trifluoromethyl)-1,3-dihydropyridin-6-one Chemical compound C1=CC(C)=CC=C1C1=C(N)C(=O)N[C@](C(F)(F)F)(C=2C=CC(OCCCC(F)(F)F)=CC=2)C1 KTEKFLCACKLBMQ-NRFANRHFSA-N 0.000 claims 1
- FBBPRPJENPWDPL-LJAQVGFWSA-N (2s)-n-(4-methoxyphenyl)-4-(4-methylphenyl)-6-oxo-2-[4-(4,4,4-trifluorobutoxy)phenyl]-2-(trifluoromethyl)-1,3-dihydropyridine-5-carboxamide Chemical compound C1=CC(OC)=CC=C1NC(=O)C1=C(C=2C=CC(C)=CC=2)C[C@@](C(F)(F)F)(C=2C=CC(OCCCC(F)(F)F)=CC=2)NC1=O FBBPRPJENPWDPL-LJAQVGFWSA-N 0.000 claims 1
- 125000000027 (C1-C10) alkoxy group Chemical group 0.000 claims 1
- 125000000008 (C1-C10) alkyl group Chemical group 0.000 claims 1
- 125000004400 (C1-C12) alkyl group Chemical group 0.000 claims 1
- 125000006570 (C5-C6) heteroaryl group Chemical group 0.000 claims 1
- 125000004206 2,2,2-trifluoroethyl group Chemical group [H]C([H])(*)C(F)(F)F 0.000 claims 1
- RANCPNIFZRWTRC-UHFFFAOYSA-N 2-methyl-4-(4-methylphenyl)-6-oxo-2-[4-(4,4,4-trifluorobutoxy)phenyl]-n-[4-(trifluoromethoxy)phenyl]-1,3-dihydropyridine-5-carboxamide Chemical compound C1=CC(C)=CC=C1C(CC(C)(NC1=O)C=2C=CC(OCCCC(F)(F)F)=CC=2)=C1C(=O)NC1=CC=C(OC(F)(F)F)C=C1 RANCPNIFZRWTRC-UHFFFAOYSA-N 0.000 claims 1
- MDRKZFDCXCGPHT-LJAQVGFWSA-N 2-methyl-n-[(2s)-4-(4-methylphenyl)-6-oxo-2-[4-(4,4,4-trifluorobutoxy)phenyl]-2-(trifluoromethyl)-1,3-dihydropyridin-5-yl]benzamide Chemical compound C1=CC(C)=CC=C1C(C[C@](NC1=O)(C=2C=CC(OCCCC(F)(F)F)=CC=2)C(F)(F)F)=C1NC(=O)C1=CC=CC=C1C MDRKZFDCXCGPHT-LJAQVGFWSA-N 0.000 claims 1
- 125000000094 2-phenylethyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])C([H])([H])* 0.000 claims 1
- CDGXTJIQOFQZAW-UHFFFAOYSA-N 4-(4-methylphenyl)-2-[4-(4,4,4-trifluorobutoxy)phenyl]-2-(trifluoromethyl)-5-[5-(trifluoromethyl)-1,3,4-oxadiazol-2-yl]-1,3-dihydropyridin-6-one Chemical compound C1=CC(C)=CC=C1C(CC(NC1=O)(C=2C=CC(OCCCC(F)(F)F)=CC=2)C(F)(F)F)=C1C1=NN=C(C(F)(F)F)O1 CDGXTJIQOFQZAW-UHFFFAOYSA-N 0.000 claims 1
- HRTGGPYYUGNMKU-UHFFFAOYSA-N 4-(4-methylphenyl)-5-(2h-tetrazol-5-yl)-2-(trifluoromethyl)-2-[1-(5,5,5-trifluoropentyl)pyrazol-4-yl]-1,3-dihydropyridin-6-one Chemical compound C1=CC(C)=CC=C1C(CC(NC1=O)(C2=CN(CCCCC(F)(F)F)N=C2)C(F)(F)F)=C1C1=NNN=N1 HRTGGPYYUGNMKU-UHFFFAOYSA-N 0.000 claims 1
- UCZLQCAFLMDIFJ-UHFFFAOYSA-N 4-(4-methylphenyl)-5-nitro-2-[4-(4,4,4-trifluorobutoxy)phenyl]-2-(trifluoromethyl)-1,3-dihydropyridin-6-one Chemical compound C1=CC(C)=CC=C1C1=C([N+]([O-])=O)C(=O)NC(C(F)(F)F)(C=2C=CC(OCCCC(F)(F)F)=CC=2)C1 UCZLQCAFLMDIFJ-UHFFFAOYSA-N 0.000 claims 1
- YTDRWNDMSGPTFZ-UHFFFAOYSA-N 5-(2-ethyltetrazol-5-yl)-4-(4-methylphenyl)-2-[4-(4,4,4-trifluorobutoxy)phenyl]-2-(trifluoromethyl)-1,3-dihydropyridin-6-one Chemical compound CCN1N=NC(C=2C(NC(CC=2C=2C=CC(C)=CC=2)(C=2C=CC(OCCCC(F)(F)F)=CC=2)C(F)(F)F)=O)=N1 YTDRWNDMSGPTFZ-UHFFFAOYSA-N 0.000 claims 1
- XBDIBIFQMJCHNJ-UHFFFAOYSA-N 5-n-(4-methoxyphenyl)-2-methyl-4-(4-methylphenyl)-6-oxo-2-n-(4,4,4-trifluorobutyl)-1,3-dihydropyridine-2,5-dicarboxamide Chemical compound C1=CC(OC)=CC=C1NC(=O)C1=C(C=2C=CC(C)=CC=2)CC(C)(C(=O)NCCCC(F)(F)F)NC1=O XBDIBIFQMJCHNJ-UHFFFAOYSA-N 0.000 claims 1
- 201000001320 Atherosclerosis Diseases 0.000 claims 1
- 229940124213 Dipeptidyl peptidase 4 (DPP IV) inhibitor Drugs 0.000 claims 1
- 208000010412 Glaucoma Diseases 0.000 claims 1
- WQZGKKKJIJFFOK-GASJEMHNSA-N Glucose Natural products OC[C@H]1OC(O)[C@H](O)[C@@H](O)[C@@H]1O WQZGKKKJIJFFOK-GASJEMHNSA-N 0.000 claims 1
- 208000035150 Hypercholesterolemia Diseases 0.000 claims 1
- 206010060378 Hyperinsulinaemia Diseases 0.000 claims 1
- 208000031226 Hyperlipidaemia Diseases 0.000 claims 1
- 206010022489 Insulin Resistance Diseases 0.000 claims 1
- 208000001145 Metabolic Syndrome Diseases 0.000 claims 1
- 208000008589 Obesity Diseases 0.000 claims 1
- 208000017442 Retinal disease Diseases 0.000 claims 1
- 206010038923 Retinopathy Diseases 0.000 claims 1
- 229940127322 Sodium-Glucose Transporter 2 Inhibitors Drugs 0.000 claims 1
- 208000006011 Stroke Diseases 0.000 claims 1
- 201000000690 abdominal obesity-metabolic syndrome Diseases 0.000 claims 1
- 230000002159 abnormal effect Effects 0.000 claims 1
- 125000003342 alkenyl group Chemical group 0.000 claims 1
- 125000004414 alkyl thio group Chemical group 0.000 claims 1
- 125000000304 alkynyl group Chemical group 0.000 claims 1
- 229940125709 anorectic agent Drugs 0.000 claims 1
- 230000000879 anti-atherosclerotic effect Effects 0.000 claims 1
- 230000001708 anti-dyslipidemic effect Effects 0.000 claims 1
- 230000001346 anti-hypertriglyceridemic effect Effects 0.000 claims 1
- 230000002253 anti-ischaemic effect Effects 0.000 claims 1
- 230000003063 anti-neuropathic effect Effects 0.000 claims 1
- 239000000883 anti-obesity agent Substances 0.000 claims 1
- 230000002769 anti-restenotic effect Effects 0.000 claims 1
- 239000003529 anticholesteremic agent Substances 0.000 claims 1
- 229940125708 antidiabetic agent Drugs 0.000 claims 1
- 239000002220 antihypertensive agent Substances 0.000 claims 1
- 229940030600 antihypertensive agent Drugs 0.000 claims 1
- 229940125710 antiobesity agent Drugs 0.000 claims 1
- 125000001797 benzyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])* 0.000 claims 1
- 230000036772 blood pressure Effects 0.000 claims 1
- 125000006297 carbonyl amino group Chemical group [H]N([*:2])C([*:1])=O 0.000 claims 1
- 125000001995 cyclobutyl group Chemical group [H]C1([H])C([H])([H])C([H])(*)C1([H])[H] 0.000 claims 1
- 125000000113 cyclohexyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])(*)C([H])([H])C1([H])[H] 0.000 claims 1
- 125000004186 cyclopropylmethyl group Chemical group [H]C([H])(*)C1([H])C([H])([H])C1([H])[H] 0.000 claims 1
- 230000003111 delayed effect Effects 0.000 claims 1
- 206010012601 diabetes mellitus Diseases 0.000 claims 1
- 125000004786 difluoromethoxy group Chemical group [H]C(F)(F)O* 0.000 claims 1
- 239000003603 dipeptidyl peptidase IV inhibitor Substances 0.000 claims 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 1
- 208000035475 disorder Diseases 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 208000004104 gestational diabetes Diseases 0.000 claims 1
- 239000008103 glucose Substances 0.000 claims 1
- 125000004995 haloalkylthio group Chemical group 0.000 claims 1
- 230000004217 heart function Effects 0.000 claims 1
- 201000001421 hyperglycemia Diseases 0.000 claims 1
- 230000003451 hyperinsulinaemic effect Effects 0.000 claims 1
- 201000008980 hyperinsulinism Diseases 0.000 claims 1
- 208000006575 hypertriglyceridemia Diseases 0.000 claims 1
- 125000004499 isoxazol-5-yl group Chemical group O1N=CC=C1* 0.000 claims 1
- 208000017169 kidney disease Diseases 0.000 claims 1
- 150000002632 lipids Chemical class 0.000 claims 1
- 125000004458 methylaminocarbonyl group Chemical group [H]N(C(*)=O)C([H])([H])[H] 0.000 claims 1
- 125000004170 methylsulfonyl group Chemical group [H]C([H])([H])S(*)(=O)=O 0.000 claims 1
- LRUJYYSATGFMAK-UHFFFAOYSA-N n-(4-cyanophenyl)-5,5-difluoro-4-(4-methylphenyl)-2-oxo-6-[4-(4,4,4-trifluorobutoxy)phenyl]-6-(trifluoromethyl)-1h-pyridine-3-carboxamide Chemical compound C1=CC(C)=CC=C1C(C(C(C=1C=CC(OCCCC(F)(F)F)=CC=1)(C(F)(F)F)NC1=O)(F)F)=C1C(=O)NC1=CC=C(C#N)C=C1 LRUJYYSATGFMAK-UHFFFAOYSA-N 0.000 claims 1
- YYUDOVKKAKHOOY-UHFFFAOYSA-N n-(4-methoxyphenyl)-4-(4-methylphenyl)-2-oxo-6-[4-(4,4,4-trifluorobutoxy)phenyl]-6-(trifluoromethyl)piperidine-3-carboxamide Chemical compound C1=CC(OC)=CC=C1NC(=O)C1C(=O)NC(C(F)(F)F)(C=2C=CC(OCCCC(F)(F)F)=CC=2)CC1C1=CC=C(C)C=C1 YYUDOVKKAKHOOY-UHFFFAOYSA-N 0.000 claims 1
- FBBPRPJENPWDPL-UHFFFAOYSA-N n-(4-methoxyphenyl)-4-(4-methylphenyl)-6-oxo-2-[4-(4,4,4-trifluorobutoxy)phenyl]-2-(trifluoromethyl)-1,3-dihydropyridine-5-carboxamide Chemical compound C1=CC(OC)=CC=C1NC(=O)C1=C(C=2C=CC(C)=CC=2)CC(C(F)(F)F)(C=2C=CC(OCCCC(F)(F)F)=CC=2)NC1=O FBBPRPJENPWDPL-UHFFFAOYSA-N 0.000 claims 1
- 125000000740 n-pentyl group Chemical group [H]C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])* 0.000 claims 1
- 201000001119 neuropathy Diseases 0.000 claims 1
- 230000007823 neuropathy Effects 0.000 claims 1
- IJGRMHOSHXDMSA-UHFFFAOYSA-N nitrogen Substances N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims 1
- 235000020824 obesity Nutrition 0.000 claims 1
- 125000003854 p-chlorophenyl group Chemical group [H]C1=C([H])C(*)=C([H])C([H])=C1Cl 0.000 claims 1
- 208000033808 peripheral neuropathy Diseases 0.000 claims 1
- 230000002265 prevention Effects 0.000 claims 1
- 125000004528 pyrimidin-5-yl group Chemical group N1=CN=CC(=C1)* 0.000 claims 1
- 125000000714 pyrimidinyl group Chemical group 0.000 claims 1
- 229920006395 saturated elastomer Polymers 0.000 claims 1
- 238000002560 therapeutic procedure Methods 0.000 claims 1
- 125000000876 trifluoromethoxy group Chemical group FC(F)(F)O* 0.000 claims 1
- 208000001072 type 2 diabetes mellitus Diseases 0.000 claims 1
- 230000029663 wound healing Effects 0.000 claims 1
Classifications
-
- 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
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/438—The ring being spiro-condensed with carbocyclic or heterocyclic ring systems
-
- 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
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/4418—Non condensed pyridines; Hydrogenated derivatives thereof having a carbocyclic group directly attached to the heterocyclic ring, e.g. cyproheptadine
-
- 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
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
-
- 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
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
- A61K31/4439—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
-
- 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
- A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
- A61K31/5375—1,4-Oxazines, e.g. morpholine
- A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
-
- 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
- A61K31/66—Phosphorus compounds
- A61K31/675—Phosphorus compounds having nitrogen as a ring hetero atom, e.g. pyridoxal phosphate
-
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US201161566039P | 2011-12-02 | 2011-12-02 | |
US13/688,584 US8791091B2 (en) | 2011-12-02 | 2012-11-29 | Aryl dihydropyridinone and piperidinone MGAT2 inhibitors |
PCT/US2012/067173 WO2013082345A1 (en) | 2011-12-02 | 2012-11-30 | Aryl dihydropyridinone and piperidinone as mgat2 inhibitors |
EP12821212.3A EP2785693B1 (en) | 2011-12-02 | 2012-11-30 | Aryl dihydropyridinones and piperidinones as mgat2 inhibitors |
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US8791091B2 (en) * | 2011-12-02 | 2014-07-29 | Bristol-Myers Squibb Company | Aryl dihydropyridinone and piperidinone MGAT2 inhibitors |
CN104918935B (zh) | 2012-11-16 | 2017-07-28 | 百时美施贵宝公司 | 二氢吡唑gpr40调节剂 |
DK2920165T3 (en) | 2012-11-16 | 2017-01-16 | Bristol Myers Squibb Co | Dihydropyrazol-GPR40-MODULATORS |
SG11201503562PA (en) | 2012-11-16 | 2015-06-29 | Bristol Myers Squibb Co | Dihydropyrazole gpr40 modulators |
CN105121426B (zh) | 2012-11-16 | 2017-03-29 | 百时美施贵宝公司 | 吡咯烷gpr40调节剂 |
NZ706418A (en) | 2012-11-29 | 2019-09-27 | Merck Patent Gmbh | Azaquinazoline carboxamide derivatives |
EP3004059B1 (en) | 2013-05-29 | 2017-09-20 | Bristol-Myers Squibb Company | Dihydropyridinone mgat2 inhibitors |
WO2015134701A1 (en) | 2014-03-07 | 2015-09-11 | Bristol-Myers Squibb Company | Dihydropyridinone mgat2 inhibitors for use in the treatment of metabolic disorders |
SI3114120T1 (sl) | 2014-03-07 | 2019-04-30 | Bristol-Myers Squibb Company | Tetrazolon-substituirani dihidropiridinon mgat2 inhibitorji |
WO2015191681A2 (en) | 2014-06-11 | 2015-12-17 | Bristol-Myers Squibb Company | Substituted pyridinones as mgat2 inhibitors |
KR101750392B1 (ko) * | 2014-12-03 | 2017-06-26 | 한국도로공사 | 교량 점검용 거더의 유도 레일장치 및 그 교량 점검장치 |
WO2017069224A1 (ja) * | 2015-10-22 | 2017-04-27 | 塩野義製薬株式会社 | Mgat2阻害活性を有するスピロ環誘導体 |
JPWO2017110841A1 (ja) * | 2015-12-21 | 2018-10-11 | 塩野義製薬株式会社 | Mgat2阻害活性を有する非芳香族複素環誘導体 |
EP3301094A1 (en) * | 2016-09-30 | 2018-04-04 | Mutabilis | Heterocyclic compounds and their use in preventing or treating bacterial infections |
JP2020158390A (ja) * | 2017-06-20 | 2020-10-01 | 塩野義製薬株式会社 | Mgat2阻害活性を有する非芳香族複素環誘導体およびそれらを含有する医薬組成物 |
TWI782056B (zh) | 2017-07-14 | 2022-11-01 | 日商鹽野義製藥股份有限公司 | 具有mgat2抑制活性的縮合環衍生物 |
CN107759498A (zh) * | 2017-11-08 | 2018-03-06 | 南京大学 | 抗肿瘤化合物、制备方法及其用途 |
AU2020207716A1 (en) | 2019-01-11 | 2021-07-15 | Shionogi & Co., Ltd. | Dihydropyrazolopyrazinone derivative having MGAT2 inhibitory activity |
JP7413346B2 (ja) | 2019-03-06 | 2024-01-15 | 第一三共株式会社 | ピロロピラゾール誘導体 |
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US3073838A (en) * | 1963-01-15 | Derivatives of hydkogenateb pyridones | ||
US5614492A (en) | 1986-05-05 | 1997-03-25 | The General Hospital Corporation | Insulinotropic hormone GLP-1 (7-36) and uses thereof |
CN101084207A (zh) | 2004-09-20 | 2007-12-05 | 泽农医药公司 | 杂环衍生物及其作为硬脂酰CoA去饱和酶抑制剂的用途 |
WO2007002191A2 (en) * | 2005-06-22 | 2007-01-04 | Biocryst Pharmaceuticals, Inc. | Methods for the preparation of 9-deazapurine derivatives |
JPWO2008038768A1 (ja) | 2006-09-28 | 2010-01-28 | 大日本住友製薬株式会社 | 二環性ピリミジン構造を有する化合物及びそれを含有する医薬組成物 |
WO2008093464A1 (ja) | 2007-01-31 | 2008-08-07 | Banyu Pharmaceutical Co., Ltd. | Mgat2遺伝子改変動物 |
AU2010216633A1 (en) | 2009-02-23 | 2011-09-08 | Msd K.K. | Pyrimidin-4(3H)-one derivatives |
US9035059B2 (en) | 2011-03-14 | 2015-05-19 | Taisho Pharmaceutical Co., Ltd. | Nitrogen-containing condensed heterocyclic compound |
US8791091B2 (en) * | 2011-12-02 | 2014-07-29 | Bristol-Myers Squibb Company | Aryl dihydropyridinone and piperidinone MGAT2 inhibitors |
SI3114120T1 (sl) | 2014-03-07 | 2019-04-30 | Bristol-Myers Squibb Company | Tetrazolon-substituirani dihidropiridinon mgat2 inhibitorji |
WO2015134701A1 (en) | 2014-03-07 | 2015-09-11 | Bristol-Myers Squibb Company | Dihydropyridinone mgat2 inhibitors for use in the treatment of metabolic disorders |
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