RU2019117556A - Индазольные производные, пригодные в качестве ингибиторов диацилглицерид o-ацилтрансферазы 2 - Google Patents
Индазольные производные, пригодные в качестве ингибиторов диацилглицерид o-ацилтрансферазы 2 Download PDFInfo
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- RU2019117556A RU2019117556A RU2019117556A RU2019117556A RU2019117556A RU 2019117556 A RU2019117556 A RU 2019117556A RU 2019117556 A RU2019117556 A RU 2019117556A RU 2019117556 A RU2019117556 A RU 2019117556A RU 2019117556 A RU2019117556 A RU 2019117556A
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- RU
- Russia
- Prior art keywords
- indazole
- cabroxamide
- fluorophenyl
- chlorophenyl
- alkyl
- Prior art date
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- BAXOFTOLAUCFNW-UHFFFAOYSA-N 1H-indazole Chemical class C1=CC=C2C=NNC2=C1 BAXOFTOLAUCFNW-UHFFFAOYSA-N 0.000 title 1
- 239000003112 inhibitor Substances 0.000 title 1
- -1 hydroxy, phenyl Chemical group 0.000 claims 181
- 125000001255 4-fluorophenyl group Chemical group [H]C1=C([H])C(*)=C([H])C([H])=C1F 0.000 claims 146
- 125000004182 2-chlorophenyl group Chemical group [H]C1=C([H])C(Cl)=C(*)C([H])=C1[H] 0.000 claims 124
- 125000000217 alkyl group Chemical group 0.000 claims 86
- 125000005842 heteroatom Chemical group 0.000 claims 45
- 229910052760 oxygen Inorganic materials 0.000 claims 45
- 229910052717 sulfur Inorganic materials 0.000 claims 45
- 229910052736 halogen Inorganic materials 0.000 claims 39
- 125000000753 cycloalkyl group Chemical group 0.000 claims 33
- 125000001072 heteroaryl group Chemical group 0.000 claims 32
- 150000002367 halogens Chemical class 0.000 claims 30
- 125000003118 aryl group Chemical group 0.000 claims 28
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims 22
- 125000000623 heterocyclic group Chemical group 0.000 claims 21
- 125000004029 hydroxymethyl group Chemical group [H]OC([H])([H])* 0.000 claims 19
- 125000006570 (C5-C6) heteroaryl group Chemical group 0.000 claims 16
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 16
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 13
- 229910052739 hydrogen Inorganic materials 0.000 claims 13
- 239000001257 hydrogen Substances 0.000 claims 13
- 125000004356 hydroxy functional group Chemical group O* 0.000 claims 13
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 claims 12
- 125000002618 bicyclic heterocycle group Chemical group 0.000 claims 9
- 125000004093 cyano group Chemical group *C#N 0.000 claims 9
- 125000005843 halogen group Chemical group 0.000 claims 9
- 125000004191 (C1-C6) alkoxy group Chemical group 0.000 claims 8
- 125000003545 alkoxy group Chemical group 0.000 claims 8
- 125000005213 alkyl heteroaryl group Chemical group 0.000 claims 8
- 150000001875 compounds Chemical class 0.000 claims 8
- 150000003839 salts Chemical class 0.000 claims 8
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 7
- 125000003349 3-pyridyl group Chemical group N1=C([H])C([*])=C([H])C([H])=C1[H] 0.000 claims 6
- 229910052757 nitrogen Inorganic materials 0.000 claims 6
- 125000004433 nitrogen atom Chemical group N* 0.000 claims 6
- 201000001320 Atherosclerosis Diseases 0.000 claims 5
- 125000006163 5-membered heteroaryl group Chemical group 0.000 claims 4
- 125000005037 alkyl phenyl group Chemical group 0.000 claims 4
- 125000004786 difluoromethoxy group Chemical group [H]C(F)(F)O* 0.000 claims 3
- 125000001436 propyl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])[H] 0.000 claims 3
- 125000004528 pyrimidin-5-yl group Chemical group N1=CN=CC(=C1)* 0.000 claims 3
- 125000004207 3-methoxyphenyl group Chemical group [H]C1=C([H])C(*)=C([H])C(OC([H])([H])[H])=C1[H] 0.000 claims 2
- 206010019708 Hepatic steatosis Diseases 0.000 claims 2
- 208000035150 Hypercholesterolemia Diseases 0.000 claims 2
- 208000031226 Hyperlipidaemia Diseases 0.000 claims 2
- KFZMGEQAYNKOFK-UHFFFAOYSA-N Isopropanol Chemical group CC(C)O KFZMGEQAYNKOFK-UHFFFAOYSA-N 0.000 claims 2
- 208000008589 Obesity Diseases 0.000 claims 2
- 125000001995 cyclobutyl group Chemical group [H]C1([H])C([H])([H])C([H])(*)C1([H])[H] 0.000 claims 2
- 125000001511 cyclopentyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])(*)C1([H])[H] 0.000 claims 2
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 2
- 239000003814 drug Substances 0.000 claims 2
- 238000000034 method Methods 0.000 claims 2
- 235000020824 obesity Nutrition 0.000 claims 2
- 125000000999 tert-butyl group Chemical group [H]C([H])([H])C(*)(C([H])([H])[H])C([H])([H])[H] 0.000 claims 2
- 208000001072 type 2 diabetes mellitus Diseases 0.000 claims 2
- 125000001401 1,2,4-triazol-4-yl group Chemical group N=1N=C([H])N([*])C=1[H] 0.000 claims 1
- 125000004200 2-methoxyethyl group Chemical group [H]C([H])([H])OC([H])([H])C([H])([H])* 0.000 claims 1
- 125000004179 3-chlorophenyl group Chemical group [H]C1=C([H])C(*)=C([H])C(Cl)=C1[H] 0.000 claims 1
- 125000004800 4-bromophenyl group Chemical group [H]C1=C([H])C(*)=C([H])C([H])=C1Br 0.000 claims 1
- 125000006283 4-chlorobenzyl group Chemical group [H]C1=C([H])C(=C([H])C([H])=C1Cl)C([H])([H])* 0.000 claims 1
- 125000004176 4-fluorobenzyl group Chemical group [H]C1=C([H])C(=C([H])C([H])=C1F)C([H])([H])* 0.000 claims 1
- 125000000339 4-pyridyl group Chemical group N1=C([H])C([H])=C([*])C([H])=C1[H] 0.000 claims 1
- 102100035762 Diacylglycerol O-acyltransferase 2 Human genes 0.000 claims 1
- 101000930020 Homo sapiens Diacylglycerol O-acyltransferase 2 Proteins 0.000 claims 1
- 241000124008 Mammalia Species 0.000 claims 1
- MPGRDAHTZGDVKH-UHFFFAOYSA-N N-(1,1-dioxothiolan-3-yl)-1-(4-fluorophenyl)-3-(1-oxidopyridin-1-ium-3-yl)indazole-6-carboxamide Chemical compound O=S1(CC(CC1)NC(=O)C1=CC=C2C(=NN(C2=C1)C1=CC=C(C=C1)F)C=1C=[N+](C=CC=1)[O-])=O MPGRDAHTZGDVKH-UHFFFAOYSA-N 0.000 claims 1
- PYFKNDZBJPPSIX-UHFFFAOYSA-N [3-(2-chlorophenyl)-1-(4-fluorophenyl)indazol-6-yl]-(3,3-dioxo-3lambda6-thia-6-azabicyclo[3.2.1]octan-6-yl)methanone Chemical compound ClC1=C(C=CC=C1)C1=NN(C2=CC(=CC=C12)C(=O)N1C2CS(CC(C1)C2)(=O)=O)C1=CC=C(C=C1)F PYFKNDZBJPPSIX-UHFFFAOYSA-N 0.000 claims 1
- 230000008485 antagonism Effects 0.000 claims 1
- 125000003917 carbamoyl group Chemical group [H]N([H])C(*)=O 0.000 claims 1
- 125000001559 cyclopropyl group Chemical group [H]C1([H])C([H])([H])C1([H])* 0.000 claims 1
- 201000010099 disease Diseases 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- HFDSCNFMHXNRDH-UHFFFAOYSA-N ethyl 1-[[3-(2-chlorophenyl)-1-(4-fluorophenyl)indazole-6-carbonyl]amino]cyclopropane-1-carboxylate Chemical compound ClC1=C(C=CC=C1)C1=NN(C2=CC(=CC=C12)C(=O)NC1(CC1)C(=O)OCC)C1=CC=C(C=C1)F HFDSCNFMHXNRDH-UHFFFAOYSA-N 0.000 claims 1
- QYDAVJXXKNPCAX-UHFFFAOYSA-N ethyl 2-[3-(2-chlorophenyl)-6-[(3-methyl-1,1-dioxothiolan-3-yl)carbamoyl]indazol-1-yl]-1,3-oxazole-4-carboxylate Chemical compound ClC1=C(C=CC=C1)C1=NN(C2=CC(=CC=C12)C(NC1(CS(CC1)(=O)=O)C)=O)C=1OC=C(N=1)C(=O)OCC QYDAVJXXKNPCAX-UHFFFAOYSA-N 0.000 claims 1
- 125000006125 ethylsulfonyl group Chemical group 0.000 claims 1
- 125000002140 imidazol-4-yl group Chemical group [H]N1C([H])=NC([*])=C1[H] 0.000 claims 1
- 125000001449 isopropyl group Chemical group [H]C([H])([H])C([H])(*)C([H])([H])[H] 0.000 claims 1
- 125000000040 m-tolyl group Chemical group [H]C1=C([H])C(*)=C([H])C(=C1[H])C([H])([H])[H] 0.000 claims 1
- 125000004184 methoxymethyl group Chemical group [H]C([H])([H])OC([H])([H])* 0.000 claims 1
- JYMVEPJMPDYEIA-UHFFFAOYSA-N methyl 1-[[3-(2-chlorophenyl)-1-(4-fluorophenyl)indazole-6-carbonyl]amino]cyclopentane-1-carboxylate Chemical compound ClC1=C(C=CC=C1)C1=NN(C2=CC(=CC=C12)C(=O)NC1(CCCC1)C(=O)OC)C1=CC=C(C=C1)F JYMVEPJMPDYEIA-UHFFFAOYSA-N 0.000 claims 1
- 125000002816 methylsulfanyl group Chemical group [H]C([H])([H])S[*] 0.000 claims 1
- 125000001147 pentyl group Chemical group C(CCCC)* 0.000 claims 1
- 239000008194 pharmaceutical composition Substances 0.000 claims 1
- 125000006514 pyridin-2-ylmethyl group Chemical group [H]C1=C([H])C([H])=C([H])C(=N1)C([H])([H])* 0.000 claims 1
- NYCVCXMSZNOGDH-UHFFFAOYSA-N pyrrolidine-1-carboxylic acid Chemical compound OC(=O)N1CCCC1 NYCVCXMSZNOGDH-UHFFFAOYSA-N 0.000 claims 1
- QWUFVCIGYZDHCD-FQEVSTJZSA-N tert-butyl (3S)-3-[[3-(2-chlorophenyl)-1-(4-fluorophenyl)indazole-6-carbonyl]amino]pyrrolidine-1-carboxylate Chemical compound ClC1=C(C=CC=C1)C1=NN(C2=CC(=CC=C12)C(=O)N[C@@H]1CN(CC1)C(=O)OC(C)(C)C)C1=CC=C(C=C1)F QWUFVCIGYZDHCD-FQEVSTJZSA-N 0.000 claims 1
- WCHZETLLPCMELH-UHFFFAOYSA-N tert-butyl 3-[[3-(2-chlorophenyl)-1-(4-fluorophenyl)indazole-6-carbonyl]amino]propanoate Chemical compound ClC1=C(C=CC=C1)C1=NN(C2=CC(=CC=C12)C(=O)NCCC(=O)OC(C)(C)C)C1=CC=C(C=C1)F WCHZETLLPCMELH-UHFFFAOYSA-N 0.000 claims 1
- VALOLBOVOFJSBX-UHFFFAOYSA-N tert-butyl 4-[1-[[3-(2-chlorophenyl)-1-(4-fluorophenyl)indazole-6-carbonyl]amino]ethyl]imidazole-1-carboxylate Chemical compound ClC1=C(C=CC=C1)C1=NN(C2=CC(=CC=C12)C(=O)NC(C)C=1N=CN(C=1)C(=O)OC(C)(C)C)C1=CC=C(C=C1)F VALOLBOVOFJSBX-UHFFFAOYSA-N 0.000 claims 1
- AHIXSNMWCQKTMS-UHFFFAOYSA-N tert-butyl 6-[[3-(2-chlorophenyl)-1-(4-fluorophenyl)indazole-6-carbonyl]amino]-1,1-dioxo-1,4-thiazepane-4-carboxylate Chemical compound ClC1=C(C=CC=C1)C1=NN(C2=CC(=CC=C12)C(=O)NC1CN(CCS(C1)(=O)=O)C(=O)OC(C)(C)C)C1=CC=C(C=C1)F AHIXSNMWCQKTMS-UHFFFAOYSA-N 0.000 claims 1
- 238000002560 therapeutic procedure Methods 0.000 claims 1
- 125000004495 thiazol-4-yl group Chemical group S1C=NC(=C1)* 0.000 claims 1
Classifications
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- C—CHEMISTRY; METALLURGY
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- C07D—HETEROCYCLIC COMPOUNDS
- C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
- C07D409/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
- C07D409/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D515/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen, oxygen, and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00
- C07D515/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen, oxygen, and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00 in which the condensed system contains two hetero rings
- C07D515/08—Bridged systems
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- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
- A61K31/415—1,2-Diazoles
- A61K31/416—1,2-Diazoles condensed with carbocyclic ring systems, e.g. indazole
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- A—HUMAN NECESSITIES
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- A61K31/42—Oxazoles
- A61K31/422—Oxazoles not condensed and containing further heterocyclic rings
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- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
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- A61K31/433—Thidiazoles
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- 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
- A61K31/4406—Non condensed pyridines; Hydrogenated derivatives thereof only substituted in position 3, e.g. zimeldine
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- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
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- A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
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- C07D231/00—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
- C07D231/54—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings condensed with carbocyclic rings or ring systems
- C07D231/56—Benzopyrazoles; Hydrogenated benzopyrazoles
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- C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
- C07D401/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
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- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
- C07D403/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
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- C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
- C07D405/12—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
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- C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
- C07D413/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
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- C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
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- C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
- C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
- C07D417/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
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- C—CHEMISTRY; METALLURGY
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- C07D417/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings
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- C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
- C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
- C07D487/04—Ortho-condensed systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D495/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
- C07D495/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
- C07D495/08—Bridged systems
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- Chemical & Material Sciences (AREA)
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- Engineering & Computer Science (AREA)
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- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Diabetes (AREA)
- Obesity (AREA)
- Hematology (AREA)
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- Endocrinology (AREA)
- Gastroenterology & Hepatology (AREA)
- Emergency Medicine (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
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Applications Claiming Priority (3)
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| US201662424066P | 2016-11-18 | 2016-11-18 | |
| US62/424,066 | 2016-11-18 | ||
| PCT/US2017/061223 WO2018093696A1 (en) | 2016-11-18 | 2017-11-13 | Indazole derivatives useful as inhibitors of diacylglyceride o-acyltransferase 2 |
Publications (2)
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| RU2019117556A true RU2019117556A (ru) | 2020-12-18 |
| RU2019117556A3 RU2019117556A3 (https=) | 2020-12-18 |
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| EP (1) | EP3541374A4 (https=) |
| JP (1) | JP2020502058A (https=) |
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| CN (1) | CN110121341A (https=) |
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| MA (1) | MA46856A (https=) |
| MX (1) | MX2019005786A (https=) |
| RU (1) | RU2019117556A (https=) |
| WO (1) | WO2018093696A1 (https=) |
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| Publication number | Priority date | Publication date | Assignee | Title |
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| MA41179A (fr) | 2014-12-19 | 2017-10-24 | Cancer Research Tech Ltd | Composés inhibiteurs de parg |
| EP4153584A1 (en) | 2020-05-18 | 2023-03-29 | Merck Sharp & Dohme LLC | Novel diacylglyceride o-acyltransferase 2 inhibitors |
| EP4225735A1 (en) * | 2020-10-08 | 2023-08-16 | Merck Sharp & Dohme LLC | Preparation of oxindole derivatives as novel diacylglyceride o-acyltransferase 2 inhibitors |
| MA61866B1 (fr) * | 2020-10-08 | 2026-02-27 | Merck Sharp & Dohme Llc | Préparation de dérivés de benzimidazolone servant de nouveaux inhibiteurs de diacylglycéride o-acyltransférase 2 |
| WO2022117882A2 (en) * | 2020-12-03 | 2022-06-09 | Domain Therapeutics | Novel par-2 inhibitors |
| JP2024501520A (ja) * | 2020-12-22 | 2024-01-12 | メルク・シャープ・アンド・ドーム・エルエルシー | 新規ジアシルグリセリドｏ－アシルトランスフェラーゼ２阻害薬としてのテトラヒドロインダゾール誘導体の調製 |
| AR128846A1 (es) | 2022-03-23 | 2024-06-19 | Ideaya Biosciences Inc | Compuestos de indazol sustituidos con piperazina como inhibidores de parg |
| AR131250A1 (es) | 2022-12-02 | 2025-02-26 | Merck Sharp & Dohme Llc | Preparación de derivados condensados de azol como nuevos inhibidores de la diacilglicerol o-aciltransferasa 2 |
| WO2025247370A1 (zh) * | 2024-06-01 | 2025-12-04 | 中国药科大学 | 双环类化合物及其医药用途 |
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| US6262040B1 (en) * | 1996-09-04 | 2001-07-17 | Pfizer Inc | Indazole derivatives and their use as inhibitors of phosphodiesterase (PDE) type IV and the production of tumor necrosis factor (TNF) |
| DE69819311T2 (de) | 1997-03-07 | 2004-07-29 | Metabasis Therapeutics Inc., San Diego | Neue benzimidazol inhibitoren der fructose-1,6-bisphosphatase |
| US6054587A (en) | 1997-03-07 | 2000-04-25 | Metabasis Therapeutics, Inc. | Indole and azaindole inhibitors of fructose-1,6-bisphosphatase |
| AU6452098A (en) | 1997-03-07 | 1998-09-22 | Metabasis Therapeutics, Inc. | Novel purine inhibitors of fructose-1,6-bisphosphatase |
| ATE246197T1 (de) | 1998-09-09 | 2003-08-15 | Metabasis Therapeutics Inc | Neue heteroaromatische fructose 1,6- bisphosphatase inhibitoren |
| WO2002008188A1 (en) | 2000-07-25 | 2002-01-31 | Merck & Co., Inc. | N-substituted indoles useful in the treatment of diabetes |
| WO2002060388A2 (en) | 2001-01-30 | 2002-08-08 | Merck & Co., Inc. | Acyl sulfamides for treatment of obesity, diabetes and lipid disorders |
| WO2008011131A2 (en) * | 2006-07-21 | 2008-01-24 | Takeda Pharmaceutical Company Limited | Amide compounds |
| DE60226063T2 (de) * | 2001-11-27 | 2009-05-20 | F. Hoffmann-La Roche Ag | Benzothiazole derivative |
| AR040241A1 (es) | 2002-06-10 | 2005-03-23 | Merck & Co Inc | Inhibidores de la 11-beta-hidroxiesteroide deshidrogrenasa 1 para el tratamiento de la diabetes obesidad y dislipidemia |
| WO2004020408A1 (en) | 2002-08-29 | 2004-03-11 | Merck & Co., Inc. | Indoles having anti-diabetic activity |
| WO2004019869A2 (en) | 2002-08-29 | 2004-03-11 | Merck & Co., Inc. | Indoles having anti-diabetic activity |
| JP2007504285A (ja) | 2003-01-17 | 2007-03-01 | メルク エンド カムパニー インコーポレーテッド | Ｎ−シクロヘキシルアミノカルボニルベンゼンスルホンアミド誘導体 |
| US7868037B2 (en) | 2004-07-14 | 2011-01-11 | Ptc Therapeutics, Inc. | Methods for treating hepatitis C |
| EP1771169A1 (en) | 2004-07-14 | 2007-04-11 | PTC Therapeutics, Inc. | Methods for treating hepatitis c |
| WO2007084413A2 (en) | 2004-07-14 | 2007-07-26 | Ptc Therapeutics, Inc. | Methods for treating hepatitis c |
| JP5080450B2 (ja) | 2005-04-30 | 2012-11-21 | ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング | 新規なピペリジン置換インドール |
| JP2009523732A (ja) | 2006-01-13 | 2009-06-25 | ピーティーシー セラピューティクス，インコーポレーテッド | Ｃ型肝炎の治療方法 |
| US7514433B2 (en) | 2006-08-03 | 2009-04-07 | Hoffmann-La Roche Inc. | 1H-indole-6-yl-piperazin-1-yl-methanone derivatives |
| WO2008088692A2 (en) | 2007-01-12 | 2008-07-24 | Merck & Co., Inc. | Spirochromanon derivatives |
| EP2174343A1 (en) | 2007-06-28 | 2010-04-14 | Semiconductor Energy Laboratory Co, Ltd. | Manufacturing method of semiconductor device |
| AU2008267724A1 (en) | 2007-06-28 | 2008-12-31 | Merck Frosst Canada Ltd | Substituted fused pyrimidines as antagonists of GPR105 activity |
| DE102007032507A1 (de) * | 2007-07-12 | 2009-04-02 | Merck Patent Gmbh | Pyridazinonderivate |
| WO2009042053A2 (en) | 2007-09-21 | 2009-04-02 | Merck & Co., Inc. | Neuromedin u receptor agonists and uses thereof |
| AU2008319309B2 (en) | 2007-10-31 | 2012-09-06 | Merck Sharp & Dohme Llc | P2X3 receptor antagonists for treatment of pain |
| CA2703909A1 (en) | 2007-10-31 | 2009-05-07 | Merck Sharp & Dohme Corp. | P2x3, receptor antagonists for treatment of pain |
| ES2534199T3 (es) | 2008-10-31 | 2015-04-20 | Merck Sharp & Dohme Corp. | Antagonistas del receptor P2X3 para el tratamiento del dolor |
| EP2210891A1 (en) * | 2009-01-26 | 2010-07-28 | Domain Therapeutics | New adenosine receptor ligands and uses thereof |
| US20120022057A1 (en) | 2009-03-18 | 2012-01-26 | Schering Corporation | Bicyclic compounds as inhibitors of diacyglycerol acyltransferase |
| US8946231B2 (en) | 2009-03-23 | 2015-02-03 | Merck Sharp & Dohme Corp. | P2X3, receptor antagonists for treatment of pain |
| AU2010229144B2 (en) * | 2009-03-23 | 2012-07-12 | Merck Sharp & Dohme Corp. | P2X3, receptor antagonists for treatment of pain |
| WO2010111058A1 (en) | 2009-03-23 | 2010-09-30 | Merck Sharp & Dohme Corp. | P2x3, receptor antagonists for treatment of pain |
| WO2010118009A1 (en) | 2009-04-06 | 2010-10-14 | Ptc Therapeutics, Inc. | Hcv inhibitor and therapeutic agent combinations |
| WO2014026329A1 (en) | 2012-08-15 | 2014-02-20 | Merck Sharp & Dohme Corp. | N-alkylated indole and indazole compounds as rorgammat inhibitors and uses thereof |
| WO2016036633A1 (en) | 2014-09-05 | 2016-03-10 | Merck Sharp & Dohme Corp. | Tetrahydroisoquinoline derivatives useful as inhibitors of diacylglyceride o-acyltransferase 2 |
| US9877957B2 (en) | 2014-09-05 | 2018-01-30 | Merck Sharp & Dohme Corp. | Tetrahydroisoquinoline derivatives useful as inhibitors of diacylglyceride O-acyltransferase 2 |
| WO2016036638A1 (en) | 2014-09-05 | 2016-03-10 | Merck Sharp & Dohme Corp. | Isoquinoline derivatives useful as inhibitors of diacylglyceride o-acyltransferase 2 |
| WO2016187384A1 (en) | 2015-05-20 | 2016-11-24 | Eli Lilly And Company | Novel dgat2 inhibitors |
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- 2017-11-13 BR BR112019010164A patent/BR112019010164A2/pt not_active IP Right Cessation
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Also Published As
| Publication number | Publication date |
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| BR112019010164A2 (pt) | 2019-09-17 |
| EP3541374A1 (en) | 2019-09-25 |
| KR20190078646A (ko) | 2019-07-04 |
| EP3541374A4 (en) | 2020-06-10 |
| MA46856A (fr) | 2019-09-25 |
| CN110121341A (zh) | 2019-08-13 |
| WO2018093696A1 (en) | 2018-05-24 |
| MX2019005786A (es) | 2019-08-26 |
| US20190330239A1 (en) | 2019-10-31 |
| RU2019117556A3 (https=) | 2020-12-18 |
| AU2017360939B2 (en) | 2022-03-03 |
| CA3043203A1 (en) | 2018-05-24 |
| JP2020502058A (ja) | 2020-01-23 |
| AU2017360939A1 (en) | 2019-05-16 |
| US11104690B2 (en) | 2021-08-31 |
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