JP2018521021A5 - - Google Patents

Info

Publication number

JP2018521021A5

JP2018521021A5 JP2017563348A JP2017563348A JP2018521021A5 JP 2018521021 A5 JP2018521021 A5 JP 2018521021A5 JP 2017563348 A JP2017563348 A JP 2017563348A JP 2017563348 A JP2017563348 A JP 2017563348A JP 2018521021 A5 JP2018521021 A5 JP 2018521021A5

Authority

JP

Japan

Prior art keywords

methyl

solvate

hydrate

pharmaceutically acceptable

acceptable salt

Prior art date

2016-06-13

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.)

Pending

Links

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• 150000001875 compounds Chemical class 0.000 claims 62
• 150000003839 salts Chemical class 0.000 claims 49
• 239000012453 solvate Substances 0.000 claims 49
• 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 37
• 229910052739 hydrogen Inorganic materials 0.000 claims 33
• 239000001257 hydrogen Substances 0.000 claims 33
• -1 cyano, hydroxyl Chemical group 0.000 claims 25
• 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 24
• 229910052799 carbon Inorganic materials 0.000 claims 22
• 125000002947 alkylene group Chemical group 0.000 claims 19
• 102100028100 Activating signal cointegrator 1 Human genes 0.000 claims 17
• 101710089542 Activating signal cointegrator 1 Proteins 0.000 claims 17
• UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 17
• 125000004432 carbon atom Chemical group C* 0.000 claims 17
• 229910052757 nitrogen Inorganic materials 0.000 claims 16
• 150000002431 hydrogen Chemical class 0.000 claims 15
• 229910052736 halogen Inorganic materials 0.000 claims 14
• 150000002367 halogens Chemical class 0.000 claims 14
• 229920006395 saturated elastomer Polymers 0.000 claims 12
• 125000004433 nitrogen atom Chemical group N* 0.000 claims 11
• 125000004076 pyridyl group Chemical group 0.000 claims 9
• AUKXFNABVHIUAC-UHFFFAOYSA-N pyrrolidin-2-ylmethylamine Chemical compound NCC1CCCN1 AUKXFNABVHIUAC-UHFFFAOYSA-N 0.000 claims 8
• 239000008194 pharmaceutical composition Substances 0.000 claims 7
• 125000004051 hexyl group Chemical group [H]C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])* 0.000 claims 6
• 125000004737 (C1-C6) haloalkoxy group Chemical group 0.000 claims 5
• 125000000171 (C1-C6) haloalkyl group Chemical group 0.000 claims 5
• 125000000882 C2-C6 alkenyl group Chemical group 0.000 claims 5
• 125000005842 heteroatom Chemical group 0.000 claims 5
• 125000000956 methoxy group Chemical group [H]C([H])([H])O* 0.000 claims 5
• 229910052717 sulfur Inorganic materials 0.000 claims 5
• 125000006570 (C5-C6) heteroaryl group Chemical group 0.000 claims 4
• 239000004599 antimicrobial Substances 0.000 claims 4
• 125000004093 cyano group Chemical group *C#N 0.000 claims 4
• 229910052760 oxygen Inorganic materials 0.000 claims 4
• 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims 4
• 125000006552 (C3-C8) cycloalkyl group Chemical group 0.000 claims 3
• 125000000623 heterocyclic group Chemical group 0.000 claims 3
• 125000004765 (C1-C4) haloalkyl group Chemical group 0.000 claims 2
• 125000006766 (C2-C6) alkynyloxy group Chemical group 0.000 claims 2
• SMNDYUVBFMFKNZ-UHFFFAOYSA-N 2-furoic acid Chemical compound OC(=O)C1=CC=CO1 SMNDYUVBFMFKNZ-UHFFFAOYSA-N 0.000 claims 2
• KXDAEFPNCMNJSK-UHFFFAOYSA-N Benzamide Chemical compound NC(=O)C1=CC=CC=C1 KXDAEFPNCMNJSK-UHFFFAOYSA-N 0.000 claims 2
• 125000003320 C2-C6 alkenyloxy group Chemical group 0.000 claims 2
• 125000003545 alkoxy group Chemical group 0.000 claims 2
• 125000000304 alkynyl group Chemical group 0.000 claims 2
• 125000002837 carbocyclic group Chemical group 0.000 claims 2
• 125000000753 cycloalkyl group Chemical group 0.000 claims 2
• 125000002541 furyl group Chemical group 0.000 claims 2
• 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 2
• 208000015181 infectious disease Diseases 0.000 claims 2
• 230000000813 microbial effect Effects 0.000 claims 2
• 125000004043 oxo group Chemical group O=* 0.000 claims 2
• NGXSWUFDCSEIOO-UHFFFAOYSA-N pyrrolidin-3-amine Chemical compound NC1CCNC1 NGXSWUFDCSEIOO-UHFFFAOYSA-N 0.000 claims 2
• 125000000335 thiazolyl group Chemical group 0.000 claims 2
• FFTVPQUHLQBXQZ-KVUCHLLUSA-N (4s,4as,5ar,12ar)-4,7-bis(dimethylamino)-1,10,11,12a-tetrahydroxy-3,12-dioxo-4a,5,5a,6-tetrahydro-4h-tetracene-2-carboxamide Chemical compound C1C2=C(N(C)C)C=CC(O)=C2C(O)=C2[C@@H]1C[C@H]1[C@H](N(C)C)C(=O)C(C(N)=O)=C(O)[C@@]1(O)C2=O FFTVPQUHLQBXQZ-KVUCHLLUSA-N 0.000 claims 1
• 125000004767 (C1-C4) haloalkoxy group Chemical group 0.000 claims 1
• 125000006643 (C2-C6) haloalkenyl group Chemical group 0.000 claims 1
• 125000004215 2,4-difluorophenyl group Chemical group [H]C1=C([H])C(*)=C(F)C([H])=C1F 0.000 claims 1
• IZXIZTKNFFYFOF-UHFFFAOYSA-N 2-Oxazolidone Chemical group O=C1NCCO1 IZXIZTKNFFYFOF-UHFFFAOYSA-N 0.000 claims 1
• 125000004182 2-chlorophenyl group Chemical group [H]C1=C([H])C(Cl)=C(*)C([H])=C1[H] 0.000 claims 1
• DPBWFNDFMCCGGJ-UHFFFAOYSA-N 4-Piperidine carboxamide Chemical compound NC(=O)C1CCNCC1 DPBWFNDFMCCGGJ-UHFFFAOYSA-N 0.000 claims 1
• 125000004800 4-bromophenyl group Chemical group [H]C1=C([H])C(*)=C([H])C([H])=C1Br 0.000 claims 1
• XMPZLAQHPIBDSO-UHFFFAOYSA-N argon dimer Chemical compound [Ar].[Ar] XMPZLAQHPIBDSO-UHFFFAOYSA-N 0.000 claims 1
• FDPKMJDUXJFKOI-UHFFFAOYSA-N azetidin-3-amine Chemical compound NC1CNC1 FDPKMJDUXJFKOI-UHFFFAOYSA-N 0.000 claims 1
• 230000003115 biocidal effect Effects 0.000 claims 1
• 125000000532 dioxanyl group Chemical group 0.000 claims 1
• 125000004438 haloalkoxy group Chemical group 0.000 claims 1
• 125000004970 halomethyl group Chemical group 0.000 claims 1
• 125000001072 heteroaryl group Chemical group 0.000 claims 1
• 150000004677 hydrates Chemical class 0.000 claims 1
• 125000004435 hydrogen atom Chemical group [H]* 0.000 claims 1
• 125000002883 imidazolyl group Chemical group 0.000 claims 1
• 125000001786 isothiazolyl group Chemical group 0.000 claims 1
• 125000000842 isoxazolyl group Chemical group 0.000 claims 1
• 229960003907 linezolid Drugs 0.000 claims 1
• TYZROVQLWOKYKF-ZDUSSCGKSA-N linezolid Chemical compound O=C1O[C@@H](CNC(=O)C)CN1C(C=C1F)=CC=C1N1CCOCC1 TYZROVQLWOKYKF-ZDUSSCGKSA-N 0.000 claims 1
• 229960004023 minocycline Drugs 0.000 claims 1
• 125000002757 morpholinyl group Chemical group 0.000 claims 1
• 125000002971 oxazolyl group Chemical group 0.000 claims 1
• 125000003854 p-chlorophenyl group Chemical group [H]C1=C([H])C(*)=C([H])C([H])=C1Cl 0.000 claims 1
• 125000000951 phenoxy group Chemical group [H]C1=C([H])C([H])=C(O*)C([H])=C1[H] 0.000 claims 1
• 229910052698 phosphorus Inorganic materials 0.000 claims 1
• 125000004193 piperazinyl group Chemical group 0.000 claims 1
• BCIIMDOZSUCSEN-UHFFFAOYSA-N piperidin-4-amine Chemical compound NC1CCNCC1 BCIIMDOZSUCSEN-UHFFFAOYSA-N 0.000 claims 1
• 125000003386 piperidinyl group Chemical group 0.000 claims 1
• 125000003373 pyrazinyl group Chemical group 0.000 claims 1
• 125000003226 pyrazolyl group Chemical group 0.000 claims 1
• 125000002098 pyridazinyl group Chemical group 0.000 claims 1
• 125000000714 pyrimidinyl group Chemical group 0.000 claims 1
• OQCUGPQOZNYIMV-UHFFFAOYSA-N pyrrolidin-3-ylmethanamine Chemical compound NCC1CCNC1 OQCUGPQOZNYIMV-UHFFFAOYSA-N 0.000 claims 1
• VLJNHYLEOZPXFW-UHFFFAOYSA-N pyrrolidine-2-carboxamide Chemical compound NC(=O)C1CCCN1 VLJNHYLEOZPXFW-UHFFFAOYSA-N 0.000 claims 1
• IQHXABCGSFAKPN-UHFFFAOYSA-N pyrrolidine-3-carboxamide Chemical compound NC(=O)C1CCNC1 IQHXABCGSFAKPN-UHFFFAOYSA-N 0.000 claims 1
• 125000000719 pyrrolidinyl group Chemical group 0.000 claims 1
• 125000000168 pyrrolyl group Chemical group 0.000 claims 1
• 239000000126 substance Substances 0.000 claims 1
• 229940072172 tetracycline antibiotic Drugs 0.000 claims 1
• 125000003718 tetrahydrofuranyl group Chemical group 0.000 claims 1
• 125000003831 tetrazolyl group Chemical group 0.000 claims 1
• 125000001544 thienyl group Chemical group 0.000 claims 1
• 125000001425 triazolyl group Chemical group 0.000 claims 1
• 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 claims 1
• XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 claims 1