JP2017520538A5 - - Google Patents
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- Publication number
- JP2017520538A5 JP2017520538A5 JP2016571149A JP2016571149A JP2017520538A5 JP 2017520538 A5 JP2017520538 A5 JP 2017520538A5 JP 2016571149 A JP2016571149 A JP 2016571149A JP 2016571149 A JP2016571149 A JP 2016571149A JP 2017520538 A5 JP2017520538 A5 JP 2017520538A5
- Authority
- JP
- Japan
- Prior art keywords
- compound
- ring
- nitrogen
- nrc
- sulfur
- Prior art date
- 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
- 150000001875 compounds Chemical class 0.000 claims 20
- IJGRMHOSHXDMSA-UHFFFAOYSA-N Atomic nitrogen Chemical compound N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims 19
- 229910052757 nitrogen Inorganic materials 0.000 claims 13
- 229910052760 oxygen Inorganic materials 0.000 claims 12
- 229910052717 sulfur Inorganic materials 0.000 claims 12
- NINIDFKCEFEMDL-UHFFFAOYSA-N Sulfur Chemical compound [S] NINIDFKCEFEMDL-UHFFFAOYSA-N 0.000 claims 11
- QVGXLLKOCUKJST-UHFFFAOYSA-N atomic oxygen Chemical compound [O] QVGXLLKOCUKJST-UHFFFAOYSA-N 0.000 claims 11
- 125000005842 heteroatom Chemical group 0.000 claims 11
- 239000001301 oxygen Substances 0.000 claims 11
- 239000011593 sulfur Substances 0.000 claims 11
- QJGQUHMNIGDVPM-UHFFFAOYSA-N nitrogen group Chemical group [N] QJGQUHMNIGDVPM-UHFFFAOYSA-N 0.000 claims 9
- 229920006395 saturated elastomer Polymers 0.000 claims 8
- 125000003118 aryl group Chemical group 0.000 claims 7
- 229910005965 SO 2 Inorganic materials 0.000 claims 6
- 150000003839 salts Chemical class 0.000 claims 6
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 5
- 229910052736 halogen Inorganic materials 0.000 claims 5
- 150000002367 halogens Chemical class 0.000 claims 5
- 125000000623 heterocyclic group Chemical group 0.000 claims 5
- 239000008194 pharmaceutical composition Substances 0.000 claims 5
- 125000004429 atom Chemical group 0.000 claims 4
- 201000010099 disease Diseases 0.000 claims 4
- 229910052739 hydrogen Inorganic materials 0.000 claims 3
- 239000001257 hydrogen Substances 0.000 claims 3
- 201000006417 multiple sclerosis Diseases 0.000 claims 3
- 125000003341 7 membered heterocyclic group Chemical group 0.000 claims 2
- 102100037602 P2X purinoceptor 7 Human genes 0.000 claims 2
- 101710189965 P2X purinoceptor 7 Proteins 0.000 claims 2
- 125000001931 aliphatic group Chemical group 0.000 claims 2
- 125000002619 bicyclic group Chemical group 0.000 claims 2
- 125000000582 cycloheptyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])([H])C([H])(*)C([H])([H])C1([H])[H] 0.000 claims 2
- 125000000113 cyclohexyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])(*)C([H])([H])C1([H])[H] 0.000 claims 2
- 206010015037 epilepsy Diseases 0.000 claims 2
- 125000001072 heteroaryl group Chemical group 0.000 claims 2
- 125000004435 hydrogen atom Chemical class [H]* 0.000 claims 2
- 125000002943 quinolinyl group Chemical group N1=C(C=CC2=CC=CC=C12)* 0.000 claims 2
- -1 —SR Chemical group 0.000 claims 2
- HDDHLRKCWLHXTN-OPILKIMUSA-N 6-chloro-n-[[(1s,3s)-1-hydroxy-3-methylcyclohexyl]methyl]-2-(3-hydroxy-3-methylpyrrolidin-1-yl)quinoline-5-carboxamide Chemical compound C1[C@@H](C)CCC[C@@]1(O)CNC(=O)C1=C(Cl)C=CC2=NC(N3CC(C)(O)CC3)=CC=C12 HDDHLRKCWLHXTN-OPILKIMUSA-N 0.000 claims 1
- BAHOQKHEWZJWME-WNSKOXEYSA-N 6-chloro-n-[[(1s,3s)-1-hydroxy-3-methylcyclohexyl]methyl]-2-(4-hydroxypiperidin-1-yl)quinoline-5-carboxamide Chemical compound C1[C@@H](C)CCC[C@@]1(O)CNC(=O)C1=C(Cl)C=CC2=NC(N3CCC(O)CC3)=CC=C12 BAHOQKHEWZJWME-WNSKOXEYSA-N 0.000 claims 1
- GTFTZKPCYSYNOU-KIMHZCHSSA-N 6-chloro-n-[[(1s,3s)-1-hydroxy-3-methylcyclohexyl]methyl]-2-[(3r)-3-hydroxypyrrolidin-1-yl]quinoline-5-carboxamide Chemical compound C1[C@@H](C)CCC[C@@]1(O)CNC(=O)C1=C(Cl)C=CC2=NC(N3C[C@H](O)CC3)=CC=C12 GTFTZKPCYSYNOU-KIMHZCHSSA-N 0.000 claims 1
- GTFTZKPCYSYNOU-DFFLPILJSA-N 6-chloro-n-[[(1s,3s)-1-hydroxy-3-methylcyclohexyl]methyl]-2-[(3s)-3-hydroxypyrrolidin-1-yl]quinoline-5-carboxamide Chemical compound C1[C@@H](C)CCC[C@@]1(O)CNC(=O)C1=C(Cl)C=CC2=NC(N3C[C@@H](O)CC3)=CC=C12 GTFTZKPCYSYNOU-DFFLPILJSA-N 0.000 claims 1
- 208000024827 Alzheimer disease Diseases 0.000 claims 1
- 208000019901 Anxiety disease Diseases 0.000 claims 1
- 201000001320 Atherosclerosis Diseases 0.000 claims 1
- 206010004446 Benign prostatic hyperplasia Diseases 0.000 claims 1
- 208000030814 Eating disease Diseases 0.000 claims 1
- 208000034347 Faecal incontinence Diseases 0.000 claims 1
- 208000019454 Feeding and Eating disease Diseases 0.000 claims 1
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 1
- 206010020751 Hypersensitivity Diseases 0.000 claims 1
- 208000022559 Inflammatory bowel disease Diseases 0.000 claims 1
- 206010026749 Mania Diseases 0.000 claims 1
- 208000018737 Parkinson disease Diseases 0.000 claims 1
- 208000004403 Prostatic Hyperplasia Diseases 0.000 claims 1
- 201000004681 Psoriasis Diseases 0.000 claims 1
- 206010039085 Rhinitis allergic Diseases 0.000 claims 1
- 208000030886 Traumatic Brain injury Diseases 0.000 claims 1
- 206010046543 Urinary incontinence Diseases 0.000 claims 1
- 206010046851 Uveitis Diseases 0.000 claims 1
- 239000002671 adjuvant Substances 0.000 claims 1
- 125000000217 alkyl group Chemical group 0.000 claims 1
- 208000026935 allergic disease Diseases 0.000 claims 1
- 201000010105 allergic rhinitis Diseases 0.000 claims 1
- 230000036506 anxiety Effects 0.000 claims 1
- 208000006673 asthma Diseases 0.000 claims 1
- 125000002393 azetidinyl group Chemical group 0.000 claims 1
- 239000012472 biological sample Substances 0.000 claims 1
- 125000002837 carbocyclic group Chemical group 0.000 claims 1
- 230000001684 chronic effect Effects 0.000 claims 1
- 208000010877 cognitive disease Diseases 0.000 claims 1
- 125000001995 cyclobutyl group Chemical group [H]C1([H])C([H])([H])C([H])(*)C1([H])[H] 0.000 claims 1
- 125000001511 cyclopentyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])(*)C1([H])[H] 0.000 claims 1
- 125000001559 cyclopropyl group Chemical group [H]C1([H])C([H])([H])C1([H])* 0.000 claims 1
- 208000035475 disorder Diseases 0.000 claims 1
- 235000014632 disordered eating Nutrition 0.000 claims 1
- 230000000694 effects Effects 0.000 claims 1
- 206010014599 encephalitis Diseases 0.000 claims 1
- 125000001188 haloalkyl group Chemical group 0.000 claims 1
- 230000009610 hypersensitivity Effects 0.000 claims 1
- 210000004072 lung Anatomy 0.000 claims 1
- 238000004519 manufacturing process Methods 0.000 claims 1
- 230000001404 mediated effect Effects 0.000 claims 1
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 1
- 125000002757 morpholinyl group Chemical group 0.000 claims 1
- 208000010125 myocardial infarction Diseases 0.000 claims 1
- 230000000414 obstructive effect Effects 0.000 claims 1
- 201000008482 osteoarthritis Diseases 0.000 claims 1
- 125000003566 oxetanyl group Chemical group 0.000 claims 1
- 125000004193 piperazinyl group Chemical group 0.000 claims 1
- 125000003386 piperidinyl group Chemical group 0.000 claims 1
- 125000000719 pyrrolidinyl group Chemical group 0.000 claims 1
- 125000001422 pyrrolinyl group Chemical group 0.000 claims 1
- 125000000168 pyrrolyl group Chemical group 0.000 claims 1
- 208000036273 reactive airway disease Diseases 0.000 claims 1
- 206010039073 rheumatoid arthritis Diseases 0.000 claims 1
- 201000000980 schizophrenia Diseases 0.000 claims 1
- 208000019116 sleep disease Diseases 0.000 claims 1
- 208000020685 sleep-wake disease Diseases 0.000 claims 1
- 125000003718 tetrahydrofuranyl group Chemical group 0.000 claims 1
- 125000001412 tetrahydropyranyl group Chemical group 0.000 claims 1
- 230000009529 traumatic brain injury Effects 0.000 claims 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201462008012P | 2014-06-05 | 2014-06-05 | |
| US62/008,012 | 2014-06-05 | ||
| PCT/US2015/034108 WO2015187905A1 (en) | 2014-06-05 | 2015-06-04 | Novel quinoline derivatives and their use in neurodegenerative diseases |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2017520538A JP2017520538A (ja) | 2017-07-27 |
| JP2017520538A5 true JP2017520538A5 (oth) | 2018-05-31 |
| JP6692759B2 JP6692759B2 (ja) | 2020-05-13 |
Family
ID=53385999
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2016571149A Expired - Fee Related JP6692759B2 (ja) | 2014-06-05 | 2015-06-04 | 新規キノリン誘導体及び神経変性疾患におけるそれらの使用 |
Country Status (9)
| Country | Link |
|---|---|
| US (2) | US9399623B2 (oth) |
| EP (1) | EP3152192A1 (oth) |
| JP (1) | JP6692759B2 (oth) |
| CN (1) | CN106573907B (oth) |
| AR (1) | AR100724A1 (oth) |
| AU (1) | AU2015269598B2 (oth) |
| CA (1) | CA2948888A1 (oth) |
| IL (1) | IL249308B (oth) |
| WO (1) | WO2015187905A1 (oth) |
Families Citing this family (8)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US8563573B2 (en) | 2007-11-02 | 2013-10-22 | Vertex Pharmaceuticals Incorporated | Azaindole derivatives as CFTR modulators |
| US8802868B2 (en) | 2010-03-25 | 2014-08-12 | Vertex Pharmaceuticals Incorporated | Solid forms of (R)-1(2,2-difluorobenzo[D][1,3]dioxo1-5-yl)-N-(1-(2,3-dihydroxypropyl-6-fluoro-2-(1-hydroxy-2-methylpropan2-yl)-1H-Indol-5-yl)-Cyclopropanecarboxamide |
| MX353408B (es) | 2010-04-22 | 2018-01-11 | Vertex Pharma | Proceso para producir compuestos de cicloalquilcarboxamido-indol. |
| RU2744460C2 (ru) | 2014-04-15 | 2021-03-09 | Вертекс Фармасьютикалз Инкорпорейтед | Фармацевтические композиции для лечения заболеваний, опосредованных муковисцидозным трансмембранным регулятором проводимости |
| WO2015187905A1 (en) * | 2014-06-05 | 2015-12-10 | Merck Patent Gmbh | Novel quinoline derivatives and their use in neurodegenerative diseases |
| US11077100B2 (en) | 2017-03-13 | 2021-08-03 | Raqualia Pharma Inc. | Tetrahydroquinoline derivatives as P2X7 receptor antagonists |
| JP7542538B2 (ja) | 2018-09-18 | 2024-08-30 | ニカング セラピューティクス， インコーポレイテッド | Ｓｒｃホモロジー－２ホスファターゼ阻害剤としての縮合三環式環誘導体 |
| CN120574171A (zh) * | 2024-03-01 | 2025-09-02 | 武汉人福创新药物研发中心有限公司 | 含sf5类喹啉衍生物及其作为p2x7拮抗剂的用途 |
Family Cites Families (11)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP1307193A1 (en) | 2000-07-27 | 2003-05-07 | Affymax Research Institute | Agonists of follicle stimulating hormone activity |
| SE0200920D0 (sv) * | 2002-03-25 | 2002-03-25 | Astrazeneca Ab | Novel compounds |
| GB0312609D0 (en) * | 2003-06-02 | 2003-07-09 | Astrazeneca Ab | Novel compounds |
| SE0302139D0 (sv) * | 2003-07-28 | 2003-07-28 | Astrazeneca Ab | Novel compounds |
| SE0402925D0 (sv) * | 2004-11-30 | 2004-11-30 | Astrazeneca Ab | Novel Compounds |
| WO2008013494A1 (en) * | 2006-07-27 | 2008-01-31 | Astrazeneca Ab | Quinoline derivatives as p2x7 receptor antagonist and their use in the treatment of rheumatoid arthritis, osteoarthritis, copd and ibd |
| JP2010520875A (ja) * | 2007-03-09 | 2010-06-17 | レノビス， インコーポレイテッド | Ｐ２ｘ７調節因子としてのビシクロヘテロアリール化合物およびその使用 |
| BRPI0809106A2 (pt) * | 2007-03-22 | 2014-08-26 | Astrazeneca Ab | Derivados de quinolina para o tratamento de doenças inflamatórias |
| US8106073B2 (en) * | 2007-11-30 | 2012-01-31 | Astrazeneca Ab | Quinoline derivatives 057 |
| CA2722035C (en) * | 2008-04-22 | 2016-10-11 | Janssen Pharmaceutica Nv | Quinoline or isoquinoline substituted p2x7 antagonists |
| WO2015187905A1 (en) * | 2014-06-05 | 2015-12-10 | Merck Patent Gmbh | Novel quinoline derivatives and their use in neurodegenerative diseases |
-
2015
- 2015-06-04 WO PCT/US2015/034108 patent/WO2015187905A1/en not_active Ceased
- 2015-06-04 AR ARP150101761A patent/AR100724A1/es unknown
- 2015-06-04 AU AU2015269598A patent/AU2015269598B2/en not_active Ceased
- 2015-06-04 US US14/730,351 patent/US9399623B2/en not_active Expired - Fee Related
- 2015-06-04 CN CN201580041824.6A patent/CN106573907B/zh not_active Expired - Fee Related
- 2015-06-04 EP EP15728739.2A patent/EP3152192A1/en not_active Withdrawn
- 2015-06-04 CA CA2948888A patent/CA2948888A1/en not_active Abandoned
- 2015-06-04 JP JP2016571149A patent/JP6692759B2/ja not_active Expired - Fee Related
-
2016
- 2016-06-21 US US15/188,301 patent/US20160296509A1/en not_active Abandoned
- 2016-11-30 IL IL249308A patent/IL249308B/en active IP Right Grant
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