CN113767090A - 三环化合物及其制备方法和医药用途 - Google Patents
三环化合物及其制备方法和医药用途 Download PDFInfo
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- CN113767090A CN113767090A CN202080032427.3A CN202080032427A CN113767090A CN 113767090 A CN113767090 A CN 113767090A CN 202080032427 A CN202080032427 A CN 202080032427A CN 113767090 A CN113767090 A CN 113767090A
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- Prior art keywords
- cycloalkyl
- alkyl
- amino
- heterocyclyl
- heteroaryl
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- 201000010099 disease Diseases 0.000 claims abstract description 25
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- 238000011282 treatment Methods 0.000 claims abstract description 16
- 230000002265 prevention Effects 0.000 claims abstract description 5
- 231100000331 toxic Toxicity 0.000 claims abstract description 5
- 230000002588 toxic effect Effects 0.000 claims abstract description 5
- -1 amino, nitro, cyano, hydroxy, mercapto Chemical class 0.000 claims description 134
- 125000000623 heterocyclic group Chemical group 0.000 claims description 65
- 125000000753 cycloalkyl group Chemical group 0.000 claims description 59
- 125000000217 alkyl group Chemical group 0.000 claims description 57
- 125000001072 heteroaryl group Chemical group 0.000 claims description 44
- 239000000203 mixture Substances 0.000 claims description 41
- 125000003118 aryl group Chemical group 0.000 claims description 40
- 229910052736 halogen Inorganic materials 0.000 claims description 40
- 150000002367 halogens Chemical class 0.000 claims description 40
- 125000003545 alkoxy group Chemical group 0.000 claims description 32
- 229910052739 hydrogen Inorganic materials 0.000 claims description 31
- 239000001257 hydrogen Substances 0.000 claims description 31
- 125000003342 alkenyl group Chemical group 0.000 claims description 29
- 125000000304 alkynyl group Chemical group 0.000 claims description 29
- 229910052757 nitrogen Inorganic materials 0.000 claims description 27
- 150000002431 hydrogen Chemical class 0.000 claims description 24
- 239000003814 drug Substances 0.000 claims description 21
- 150000003839 salts Chemical class 0.000 claims description 21
- 229910052799 carbon Inorganic materials 0.000 claims description 17
- 229910052760 oxygen Inorganic materials 0.000 claims description 17
- 239000000651 prodrug Substances 0.000 claims description 17
- 229940002612 prodrug Drugs 0.000 claims description 17
- 238000000034 method Methods 0.000 claims description 16
- 125000004043 oxo group Chemical group O=* 0.000 claims description 16
- 239000000126 substance Substances 0.000 claims description 15
- 125000002915 carbonyl group Chemical group [*:2]C([*:1])=O 0.000 claims description 14
- 150000003254 radicals Chemical class 0.000 claims description 14
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- 206010010744 Conjunctivitis allergic Diseases 0.000 claims description 10
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- 208000024998 atopic conjunctivitis Diseases 0.000 claims description 10
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- 206010046851 Uveitis Diseases 0.000 claims description 8
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims description 8
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- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims description 7
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- 208000008589 Obesity Diseases 0.000 claims description 7
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- 206010013774 Dry eye Diseases 0.000 claims description 6
- 208000010643 digestive system disease Diseases 0.000 claims description 6
- 239000003937 drug carrier Substances 0.000 claims description 6
- 125000001188 haloalkyl group Chemical group 0.000 claims description 6
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- 201000011510 cancer Diseases 0.000 claims description 5
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- 125000004438 haloalkoxy group Chemical group 0.000 claims description 5
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- 125000004737 (C1-C6) haloalkoxy group Chemical group 0.000 claims description 4
- 125000001313 C5-C10 heteroaryl group Chemical group 0.000 claims description 4
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- 125000005843 halogen group Chemical group 0.000 claims description 4
- NXPHGHWWQRMDIA-UHFFFAOYSA-M magnesium;carbanide;bromide Chemical compound [CH3-].[Mg+2].[Br-] NXPHGHWWQRMDIA-UHFFFAOYSA-M 0.000 claims description 4
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims description 4
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- 238000003756 stirring Methods 0.000 description 16
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- YNAVUWVOSKDBBP-UHFFFAOYSA-N Morpholine Chemical compound C1COCCN1 YNAVUWVOSKDBBP-UHFFFAOYSA-N 0.000 description 14
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- 241001465754 Metazoa Species 0.000 description 13
- 125000004432 carbon atom Chemical group C* 0.000 description 13
- 125000006413 ring segment Chemical group 0.000 description 13
- 125000001424 substituent group Chemical group 0.000 description 13
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- 125000002619 bicyclic group Chemical group 0.000 description 11
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- QVGXLLKOCUKJST-UHFFFAOYSA-N atomic oxygen Chemical compound [O] QVGXLLKOCUKJST-UHFFFAOYSA-N 0.000 description 10
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- 231100000027 toxicology Toxicity 0.000 description 1
- 125000000026 trimethylsilyl group Chemical group [H]C([H])([H])[Si]([*])(C([H])([H])[H])C([H])([H])[H] 0.000 description 1
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- C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
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- 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
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- C07D317/44—Heterocyclic compounds containing five-membered rings having two oxygen atoms as the only ring hetero atoms having the hetero atoms in positions 1 and 3 ortho- or peri-condensed with carbocyclic rings or ring systems
- C07D317/70—Heterocyclic compounds containing five-membered rings having two oxygen atoms as the only ring hetero atoms having the hetero atoms in positions 1 and 3 ortho- or peri-condensed with carbocyclic rings or ring systems condensed with ring systems containing two or more relevant rings
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- C07D319/22—1,4-Dioxanes; Hydrogenated 1,4-dioxanes condensed with carbocyclic rings or ring systems condensed with one naphthalene or hydrogenated naphthalene ring system
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Abstract
一种通式(I)所示的三环化合物,含有其的药物组合物,及其制备方法和医药用途被公开。该化合物可用于预防和治疗由毒性醛引发的多种疾病。
Description
PCT国内申请,说明书已公开。
Claims (9)
- PCT国内申请,权利要求书已公开。
Applications Claiming Priority (3)
Application Number | Priority Date | Filing Date | Title |
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CN2019113918885 | 2019-12-30 | ||
CN201911391888 | 2019-12-30 | ||
PCT/CN2020/140710 WO2021136244A1 (zh) | 2019-12-30 | 2020-12-29 | 三环化合物及其制备方法和医药用途 |
Publications (2)
Publication Number | Publication Date |
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CN113767090A true CN113767090A (zh) | 2021-12-07 |
CN113767090B CN113767090B (zh) | 2024-05-28 |
Family
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CN202080032427.3A Active CN113767090B (zh) | 2019-12-30 | 2020-12-29 | 三环化合物及其制备方法和医药用途 |
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US (1) | US20230021669A1 (zh) |
EP (1) | EP4086241A4 (zh) |
JP (1) | JP2023507900A (zh) |
KR (1) | KR20220122978A (zh) |
CN (1) | CN113767090B (zh) |
AU (1) | AU2020419515A1 (zh) |
CA (1) | CA3159453A1 (zh) |
TW (1) | TW202138362A (zh) |
WO (1) | WO2021136244A1 (zh) |
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WO2022267930A1 (zh) * | 2021-06-25 | 2022-12-29 | 中国医药研究开发中心有限公司 | 三环化合物及其制备方法和医药用途 |
Citations (1)
Publication number | Priority date | Publication date | Assignee | Title |
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CN108135867A (zh) * | 2015-08-21 | 2018-06-08 | 奥尔德拉医疗公司 | 醛结合物和其用途 |
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Publication number | Priority date | Publication date | Assignee | Title |
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US7973025B2 (en) * | 2005-05-26 | 2011-07-05 | Neuron Systems, Inc. | Compositions and methods of treating retinal disease |
CN117045653A (zh) * | 2013-01-23 | 2023-11-14 | 奥尔德拉医疗公司 | 与毒性醛相关的疾病和治疗 |
US10111862B2 (en) * | 2013-01-25 | 2018-10-30 | Aldeyra Therapeutics, Inc. | Traps in the treatment of macular degeneration |
BR112018003250A2 (pt) * | 2015-08-21 | 2018-09-25 | Aldeyra Therapeutics Inc | compostos deuterados e usos dos mesmos |
WO2018039197A1 (en) * | 2016-08-22 | 2018-03-01 | Aldeyra Therapeutics, Inc. | Aldehyde trapping compounds and methods of use thereof |
US20180050989A1 (en) * | 2016-08-22 | 2018-02-22 | Aldeyra Therapeutics, Inc. | Aldehyde trapping compounds and uses thereof |
-
2020
- 2020-12-29 CA CA3159453A patent/CA3159453A1/en active Pending
- 2020-12-29 WO PCT/CN2020/140710 patent/WO2021136244A1/zh unknown
- 2020-12-29 US US17/756,626 patent/US20230021669A1/en active Pending
- 2020-12-29 KR KR1020227017791A patent/KR20220122978A/ko unknown
- 2020-12-29 EP EP20909307.9A patent/EP4086241A4/en active Pending
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- 2020-12-29 JP JP2022531565A patent/JP2023507900A/ja active Pending
- 2020-12-29 CN CN202080032427.3A patent/CN113767090B/zh active Active
- 2020-12-30 TW TW109146898A patent/TW202138362A/zh unknown
Patent Citations (1)
Publication number | Priority date | Publication date | Assignee | Title |
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CN108135867A (zh) * | 2015-08-21 | 2018-06-08 | 奥尔德拉医疗公司 | 醛结合物和其用途 |
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KR20220122978A (ko) | 2022-09-05 |
EP4086241A1 (en) | 2022-11-09 |
WO2021136244A1 (zh) | 2021-07-08 |
JP2023507900A (ja) | 2023-02-28 |
AU2020419515A1 (en) | 2022-05-19 |
TW202138362A (zh) | 2021-10-16 |
CA3159453A1 (en) | 2021-07-08 |
EP4086241A4 (en) | 2024-02-07 |
CN113767090B (zh) | 2024-05-28 |
US20230021669A1 (en) | 2023-01-26 |
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