JP2018536653A5 - - Google Patents

Info

Publication number

JP2018536653A5

JP2018536653A5 JP2018522540A JP2018522540A JP2018536653A5 JP 2018536653 A5 JP2018536653 A5 JP 2018536653A5 JP 2018522540 A JP2018522540 A JP 2018522540A JP 2018522540 A JP2018522540 A JP 2018522540A JP 2018536653 A5 JP2018536653 A5 JP 2018536653A5

Authority

JP

Japan

Prior art keywords

carboxylate

piperidin

salt

compound

ethyl

Prior art date

2016-11-02

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

• 150000003839 salts Chemical class 0.000 claims 19
• 150000001875 compounds Chemical class 0.000 claims 18
• RWTNPBWLLIMQHL-UHFFFAOYSA-N fexofenadine Chemical compound C1=CC(C(C)(C(O)=O)C)=CC=C1C(O)CCCN1CCC(C(O)(C=2C=CC=CC=2)C=2C=CC=CC=2)CC1 RWTNPBWLLIMQHL-UHFFFAOYSA-N 0.000 claims 14
• 125000001183 hydrocarbyl group Chemical group 0.000 claims 9
• -1 cyano, hydroxy Chemical group 0.000 claims 5
• 229910052760 oxygen Inorganic materials 0.000 claims 5
• 229910052717 sulfur Inorganic materials 0.000 claims 5
• 208000002193 Pain Diseases 0.000 claims 4
• 125000002029 aromatic hydrocarbon group Chemical group 0.000 claims 4
• 125000004432 carbon atom Chemical group C* 0.000 claims 4
• ZDAVQPOSWCQTLX-UHFFFAOYSA-N ethyl 2-ethylheptanoate Chemical compound CCCCCC(CC)C(=O)OCC ZDAVQPOSWCQTLX-UHFFFAOYSA-N 0.000 claims 4
• 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims 4
• 125000001153 fluoro group Chemical group F* 0.000 claims 4
• 125000005842 heteroatom Chemical group 0.000 claims 4
• 229910052757 nitrogen Inorganic materials 0.000 claims 4
• PXGOKWXKJXAPGV-UHFFFAOYSA-N Fluorine Chemical compound FF PXGOKWXKJXAPGV-UHFFFAOYSA-N 0.000 claims 3
• 230000001154 acute effect Effects 0.000 claims 3
• 230000001684 chronic effect Effects 0.000 claims 3
• 239000003814 drug Substances 0.000 claims 3
• 229910052731 fluorine Inorganic materials 0.000 claims 3
• 239000011737 fluorine Substances 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
• 230000002981 neuropathic effect Effects 0.000 claims 3
• 206010012335 Dependence Diseases 0.000 claims 2
• 208000016285 Movement disease Diseases 0.000 claims 2
• NQRYJNQNLNOLGT-UHFFFAOYSA-N Piperidine Chemical compound C1CCNCC1 NQRYJNQNLNOLGT-UHFFFAOYSA-N 0.000 claims 2
• 208000010877 cognitive disease Diseases 0.000 claims 2
• 230000002757 inflammatory effect Effects 0.000 claims 2
• 125000001449 isopropyl group Chemical group [H]C([H])([H])C([H])(*)C([H])([H])[H] 0.000 claims 2
• 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 2
• 125000001436 propyl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])[H] 0.000 claims 2
• KZKRRZFCAYOXQE-UHFFFAOYSA-N 1$l^{2}-azinane Chemical compound C1CC[N]CC1 KZKRRZFCAYOXQE-UHFFFAOYSA-N 0.000 claims 1
• ULFNAOHBWGRYLW-UHFFFAOYSA-N 1-cyclononylazonane Chemical group C1CCCCCCCC1N1CCCCCCCC1 ULFNAOHBWGRYLW-UHFFFAOYSA-N 0.000 claims 1
• QUIJMHDIAFOPRK-UHFFFAOYSA-N 1-cyclooctylazocane Chemical compound C1CCCCCCC1N1CCCCCCC1 QUIJMHDIAFOPRK-UHFFFAOYSA-N 0.000 claims 1
• 125000000530 1-propynyl group Chemical group [H]C([H])([H])C#C* 0.000 claims 1
• PSNDWZOXFDKLLH-UHFFFAOYSA-N 2-azaspiro[3.4]octane Chemical compound C1NCC11CCCC1 PSNDWZOXFDKLLH-UHFFFAOYSA-N 0.000 claims 1
• NVZWMJWMTWOVNJ-UHFFFAOYSA-N 6-azaspiro[3.4]octane Chemical group C1CCC21CNCC2 NVZWMJWMTWOVNJ-UHFFFAOYSA-N 0.000 claims 1
• 208000024827 Alzheimer disease Diseases 0.000 claims 1
• 208000000094 Chronic Pain Diseases 0.000 claims 1
• 206010065390 Inflammatory pain Diseases 0.000 claims 1
• 208000009829 Lewy Body Disease Diseases 0.000 claims 1
• 201000002832 Lewy body dementia Diseases 0.000 claims 1
• 208000028017 Psychotic disease Diseases 0.000 claims 1
• 208000005298 acute pain Diseases 0.000 claims 1
• 125000003545 alkoxy group Chemical group 0.000 claims 1
• HSFWRNGVRCDJHI-UHFFFAOYSA-N alpha-acetylene Natural products C#C HSFWRNGVRCDJHI-UHFFFAOYSA-N 0.000 claims 1
• ZSIQJIWKELUFRJ-UHFFFAOYSA-N azepane Chemical compound C1CCCNCC1 ZSIQJIWKELUFRJ-UHFFFAOYSA-N 0.000 claims 1
• 125000000484 butyl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])C([H])([H])[H] 0.000 claims 1
• 229910052799 carbon Inorganic materials 0.000 claims 1
• 230000001149 cognitive effect Effects 0.000 claims 1
• 125000004093 cyano group Chemical group *C#N 0.000 claims 1
• 125000004122 cyclic group Chemical group 0.000 claims 1
• 230000000694 effects Effects 0.000 claims 1
• JNMRXPADXOICLQ-UHFFFAOYSA-N ethyl 2-[4-(N-methoxy-C-propylcarbonimidoyl)piperidin-1-yl]-6-azaspiro[3.4]octane-6-carboxylate Chemical compound CON=C(CCC)C1CCN(CC1)C1CC2(C1)CN(CC2)C(=O)OCC JNMRXPADXOICLQ-UHFFFAOYSA-N 0.000 claims 1
• 125000002534 ethynyl group Chemical group [H]C#C* 0.000 claims 1
• 229910052736 halogen Inorganic materials 0.000 claims 1
• 150000002367 halogens Chemical class 0.000 claims 1
• 125000000959 isobutyl group Chemical group [H]C([H])([H])C([H])(C([H])([H])[H])C([H])([H])* 0.000 claims 1
• 125000000956 methoxy group Chemical group [H]C([H])([H])O* 0.000 claims 1
• 125000002950 monocyclic group Chemical group 0.000 claims 1
• 230000003551 muscarinic effect Effects 0.000 claims 1
• 208000004296 neuralgia Diseases 0.000 claims 1
• 208000021722 neuropathic pain Diseases 0.000 claims 1
• 239000008194 pharmaceutical composition Substances 0.000 claims 1
• 239000000546 pharmaceutical excipient Substances 0.000 claims 1
• 208000020016 psychiatric disease Diseases 0.000 claims 1
• 239000000018 receptor agonist Substances 0.000 claims 1
• 229940044601 receptor agonist Drugs 0.000 claims 1
• 229930195734 saturated hydrocarbon Natural products 0.000 claims 1
• 201000000980 schizophrenia Diseases 0.000 claims 1
• 0 CC1*N(C)*1 Chemical compound CC1*N(C)*1 0.000 description 2