JP2018521995A5 - - Google Patents

Info

Publication number

JP2018521995A5

JP2018521995A5 JP2017566402A JP2017566402A JP2018521995A5 JP 2018521995 A5 JP2018521995 A5 JP 2018521995A5 JP 2017566402 A JP2017566402 A JP 2017566402A JP 2017566402 A JP2017566402 A JP 2017566402A JP 2018521995 A5 JP2018521995 A5 JP 2018521995A5

Authority

JP

Japan

Prior art keywords

pharmaceutical composition

drinking water

medicinal

obtainable

isoxazoline

Prior art date

2016-06-22

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

Links

• Espacenet
• Global Dossier
• Discuss

• 239000008194 pharmaceutical composition Substances 0.000 claims 22
• 239000003651 drinking water Substances 0.000 claims 20
• 235000020188 drinking water Nutrition 0.000 claims 20
• -1 methoxyethyl Chemical group 0.000 claims 20
• 238000000034 method Methods 0.000 claims 10
• GVJHHUAWPYXKBD-UHFFFAOYSA-N (±)-α-Tocopherol Chemical compound OC1=C(C)C(C)=C2OC(CCCC(C)CCCC(C)CCCC(C)C)(C)CCC2=C1C GVJHHUAWPYXKBD-UHFFFAOYSA-N 0.000 claims 8
• 241001465754 Metazoa Species 0.000 claims 7
• 238000004519 manufacturing process Methods 0.000 claims 7
• 230000003071 parasitic effect Effects 0.000 claims 7
• WEQPBCSPRXFQQS-UHFFFAOYSA-N 4,5-dihydro-1,2-oxazole Chemical compound C1CC=NO1 WEQPBCSPRXFQQS-UHFFFAOYSA-N 0.000 claims 6
• 244000045947 parasite Species 0.000 claims 6
• XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 claims 6
• 229930003427 Vitamin E Natural products 0.000 claims 4
• WIGCFUFOHFEKBI-UHFFFAOYSA-N gamma-tocopherol Natural products CC(C)CCCC(C)CCCC(C)CCCC1CCC2C(C)C(O)C(C)C(C)C2O1 WIGCFUFOHFEKBI-UHFFFAOYSA-N 0.000 claims 4
• 230000002265 prevention Effects 0.000 claims 4
• 229940046009 vitamin E Drugs 0.000 claims 4
• 239000011709 vitamin E Substances 0.000 claims 4
• 235000019165 vitamin E Nutrition 0.000 claims 4
• 238000007865 diluting Methods 0.000 claims 3
• 239000003814 drug Substances 0.000 claims 3
• 229910052736 halogen Inorganic materials 0.000 claims 3
• 150000002367 halogens Chemical class 0.000 claims 3
• 229910052739 hydrogen Inorganic materials 0.000 claims 3
• 239000001257 hydrogen Substances 0.000 claims 3
• 125000004435 hydrogen atom Chemical class [H]* 0.000 claims 3
• 241000238421 Arthropoda Species 0.000 claims 2
• 125000000217 alkyl group Chemical group 0.000 claims 2
• OSVXSBDYLRYLIG-UHFFFAOYSA-N dioxidochlorine(.) Chemical compound O=Cl=O OSVXSBDYLRYLIG-UHFFFAOYSA-N 0.000 claims 2
• 125000005745 ethoxymethyl group Chemical group [H]C([H])([H])C([H])([H])OC([H])([H])* 0.000 claims 2
• 125000001188 haloalkyl group Chemical group 0.000 claims 2
• 125000004970 halomethyl group Chemical group 0.000 claims 2
• WQYVRQLZKVEZGA-UHFFFAOYSA-N hypochlorite Chemical group Cl[O-] WQYVRQLZKVEZGA-UHFFFAOYSA-N 0.000 claims 2
• 125000004184 methoxymethyl group Chemical group [H]C([H])([H])OC([H])([H])* 0.000 claims 2
• 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 2
• 125000005767 propoxymethyl group Chemical group [H]C([H])([H])C([H])([H])C([H])([H])[#8]C([H])([H])* 0.000 claims 2
• 239000002904 solvent Substances 0.000 claims 2
• GVJHHUAWPYXKBD-IEOSBIPESA-N (R)-alpha-Tocopherol Natural products OC1=C(C)C(C)=C2O[C@@](CCC[C@H](C)CCC[C@H](C)CCCC(C)C)(C)CCC2=C1C GVJHHUAWPYXKBD-IEOSBIPESA-N 0.000 claims 1
• FLEFKKUZMDEUIP-QFIPXVFZSA-N 1-[6-[(5s)-5-(3,5-dichloro-4-fluorophenyl)-5-(trifluoromethyl)-4h-1,2-oxazol-3-yl]spiro[1h-2-benzofuran-3,3'-azetidine]-1'-yl]-2-methylsulfonylethanone Chemical compound C1N(C(=O)CS(=O)(=O)C)CC21C1=CC=C(C=3C[C@](ON=3)(C=3C=C(Cl)C(F)=C(Cl)C=3)C(F)(F)F)C=C1CO2 FLEFKKUZMDEUIP-QFIPXVFZSA-N 0.000 claims 1
• HDKWFBCPLKNOCK-SFHVURJKSA-N 3-methyl-n-[2-oxo-2-(2,2,2-trifluoroethylamino)ethyl]-5-[(5s)-5-(3,4,5-trichlorophenyl)-5-(trifluoromethyl)-4h-1,2-oxazol-3-yl]thiophene-2-carboxamide Chemical compound S1C(C(=O)NCC(=O)NCC(F)(F)F)=C(C)C=C1C1=NO[C@](C(F)(F)F)(C=2C=C(Cl)C(Cl)=C(Cl)C=2)C1 HDKWFBCPLKNOCK-SFHVURJKSA-N 0.000 claims 1
• OXDDDHGGRFRLEE-UHFFFAOYSA-N 4-[5-[3-chloro-5-(trifluoromethyl)phenyl]-5-(trifluoromethyl)-4h-1,2-oxazol-3-yl]-n-[2-oxo-2-(2,2,2-trifluoroethylamino)ethyl]naphthalene-1-carboxamide Chemical compound C12=CC=CC=C2C(C(=O)NCC(=O)NCC(F)(F)F)=CC=C1C(C1)=NOC1(C(F)(F)F)C1=CC(Cl)=CC(C(F)(F)F)=C1 OXDDDHGGRFRLEE-UHFFFAOYSA-N 0.000 claims 1
• 239000004155 Chlorine dioxide Substances 0.000 claims 1
• 206010061217 Infestation Diseases 0.000 claims 1
• 229960000982 afoxolaner Drugs 0.000 claims 1
• 125000004686 alkyl sulfanyl alkyl group Chemical group 0.000 claims 1
• 125000004390 alkyl sulfonyl group Chemical group 0.000 claims 1
• 229940087168 alpha tocopherol Drugs 0.000 claims 1
• 125000002619 bicyclic group Chemical group 0.000 claims 1
• 125000003917 carbamoyl group Chemical group [H]N([H])C(*)=O 0.000 claims 1
• 230000015556 catabolic process Effects 0.000 claims 1
• 235000019398 chlorine dioxide Nutrition 0.000 claims 1
• 150000001875 compounds Chemical class 0.000 claims 1
• 239000006184 cosolvent Substances 0.000 claims 1
• 125000004093 cyano group Chemical group *C#N 0.000 claims 1
• 125000000753 cycloalkyl group Chemical group 0.000 claims 1
• 125000006255 cyclopropyl carbonyl group Chemical group [H]C1([H])C([H])([H])C1([H])C(*)=O 0.000 claims 1
• 238000006731 degradation reaction Methods 0.000 claims 1
• 238000010790 dilution Methods 0.000 claims 1
• 239000012895 dilution Substances 0.000 claims 1
• 229940079593 drug Drugs 0.000 claims 1
• 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims 1
• 125000004672 ethylcarbonyl group Chemical group [H]C([H])([H])C([H])([H])C(*)=O 0.000 claims 1
• MLBZKOGAMRTSKP-UHFFFAOYSA-N fluralaner Chemical compound C1=C(C(=O)NCC(=O)NCC(F)(F)F)C(C)=CC(C=2CC(ON=2)(C=2C=C(Cl)C=C(Cl)C=2)C(F)(F)F)=C1 MLBZKOGAMRTSKP-UHFFFAOYSA-N 0.000 claims 1
• 229960004498 fluralaner Drugs 0.000 claims 1
• 229920005555 halobutyl Polymers 0.000 claims 1
• 125000004968 halobutyl group Chemical group 0.000 claims 1
• 125000004969 haloethyl group Chemical group 0.000 claims 1
• 229950002303 lotilaner Drugs 0.000 claims 1
• 125000001160 methoxycarbonyl group Chemical group [H]C([H])([H])OC(*)=O 0.000 claims 1
• 125000004674 methylcarbonyl group Chemical group CC(=O)* 0.000 claims 1
• 239000000203 mixture Substances 0.000 claims 1
• 230000001590 oxidative effect Effects 0.000 claims 1
• 238000002360 preparation method Methods 0.000 claims 1
• 125000004673 propylcarbonyl group Chemical group 0.000 claims 1
• 238000011012 sanitization Methods 0.000 claims 1
• 229960005393 sarolaner Drugs 0.000 claims 1
• 125000001424 substituent group Chemical group 0.000 claims 1
• 125000003718 tetrahydrofuranyl group Chemical group 0.000 claims 1
• 229960000984 tocofersolan Drugs 0.000 claims 1
• 239000002076 α-tocopherol Substances 0.000 claims 1
• 235000004835 α-tocopherol Nutrition 0.000 claims 1
• 125000001020 α-tocopherol group Chemical group 0.000 claims 1
• 0 *Cc1ccccn1 Chemical compound *Cc1ccccn1 0.000 description 2
• XNTFQMKXUFFUQO-UHFFFAOYSA-N C[n]1nccc1CN Chemical compound C[n]1nccc1CN XNTFQMKXUFFUQO-UHFFFAOYSA-N 0.000 description 1
• HRVLXTZHPZXHTR-UHFFFAOYSA-N NC1(CC1)c1ccccn1 Chemical compound NC1(CC1)c1ccccn1 HRVLXTZHPZXHTR-UHFFFAOYSA-N 0.000 description 1
• FVLAYJRLBLHIPV-UHFFFAOYSA-N Nc1cncnc1 Chemical compound Nc1cncnc1 FVLAYJRLBLHIPV-UHFFFAOYSA-N 0.000 description 1