JP2017508733A5 - - Google Patents
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- Publication number
- JP2017508733A5 JP2017508733A5 JP2016550583A JP2016550583A JP2017508733A5 JP 2017508733 A5 JP2017508733 A5 JP 2017508733A5 JP 2016550583 A JP2016550583 A JP 2016550583A JP 2016550583 A JP2016550583 A JP 2016550583A JP 2017508733 A5 JP2017508733 A5 JP 2017508733A5
- Authority
- JP
- Japan
- Prior art keywords
- formula
- compound
- hydrogen
- halogen
- alkyl
- 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
- 229910052739 hydrogen Inorganic materials 0.000 claims description 16
- 239000001257 hydrogen Substances 0.000 claims description 16
- 229910052736 halogen Inorganic materials 0.000 claims description 15
- 150000002367 halogens Chemical class 0.000 claims description 12
- 150000002431 hydrogen Chemical class 0.000 claims description 12
- -1 dehydrogen Chemical class 0.000 claims description 8
- 125000000753 cycloalkyl group Chemical group 0.000 claims description 4
- WTKZEGDFNFYCGP-UHFFFAOYSA-N Pyrazole Chemical compound C=1C=NNC=1 WTKZEGDFNFYCGP-UHFFFAOYSA-N 0.000 claims description 3
- 125000001153 fluoro group Chemical group F* 0.000 claims description 3
- 125000005843 halogen group Chemical group 0.000 claims description 3
- 150000001875 compounds Chemical class 0.000 claims 17
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 claims 7
- 125000003545 alkoxy group Chemical group 0.000 claims 6
- 125000001028 difluoromethyl group Chemical group [H]C(F)(F)* 0.000 claims 5
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 claims 5
- 201000010099 disease Diseases 0.000 claims 4
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 4
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 4
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 3
- RWRDLPDLKQPQOW-UHFFFAOYSA-N Pyrrolidine Chemical compound C1CCNC1 RWRDLPDLKQPQOW-UHFFFAOYSA-N 0.000 claims 3
- 125000000217 alkyl group Chemical group 0.000 claims 3
- 125000004216 fluoromethyl group Chemical group [H]C([H])(F)* 0.000 claims 3
- 125000000623 heterocyclic group Chemical group 0.000 claims 3
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 claims 2
- YNAVUWVOSKDBBP-UHFFFAOYSA-N Morpholine Chemical compound C1COCCN1 YNAVUWVOSKDBBP-UHFFFAOYSA-N 0.000 claims 2
- 208000002193 Pain Diseases 0.000 claims 2
- NQRYJNQNLNOLGT-UHFFFAOYSA-N Piperidine Chemical compound C1CCNCC1 NQRYJNQNLNOLGT-UHFFFAOYSA-N 0.000 claims 2
- 125000003118 aryl group Chemical group 0.000 claims 2
- 229910052731 fluorine Chemical group 0.000 claims 2
- 239000011737 fluorine Chemical group 0.000 claims 2
- 125000004433 nitrogen atom Chemical group N* 0.000 claims 2
- 150000003839 salts Chemical class 0.000 claims 2
- UWYZHKAOTLEWKK-UHFFFAOYSA-N 1,2,3,4-tetrahydroisoquinoline Chemical group C1=CC=C2CNCCC2=C1 UWYZHKAOTLEWKK-UHFFFAOYSA-N 0.000 claims 1
- 125000004105 2-pyridyl group Chemical group N1=C([*])C([H])=C([H])C([H])=C1[H] 0.000 claims 1
- 125000004070 6 membered heterocyclic group Chemical group 0.000 claims 1
- KXDAEFPNCMNJSK-UHFFFAOYSA-N Benzamide Chemical group NC(=O)C1=CC=CC=C1 KXDAEFPNCMNJSK-UHFFFAOYSA-N 0.000 claims 1
- 208000006545 Chronic Obstructive Pulmonary Disease Diseases 0.000 claims 1
- 208000000094 Chronic Pain Diseases 0.000 claims 1
- 206010012289 Dementia Diseases 0.000 claims 1
- PXGOKWXKJXAPGV-UHFFFAOYSA-N Fluorine Chemical group FF PXGOKWXKJXAPGV-UHFFFAOYSA-N 0.000 claims 1
- 206010019668 Hepatic fibrosis Diseases 0.000 claims 1
- 206010028980 Neoplasm Diseases 0.000 claims 1
- 208000036110 Neuroinflammatory disease Diseases 0.000 claims 1
- 102100037602 P2X purinoceptor 7 Human genes 0.000 claims 1
- 101710189965 P2X purinoceptor 7 Proteins 0.000 claims 1
- NINIDFKCEFEMDL-UHFFFAOYSA-N Sulfur Chemical compound [S] NINIDFKCEFEMDL-UHFFFAOYSA-N 0.000 claims 1
- 208000027418 Wounds and injury Diseases 0.000 claims 1
- QVGXLLKOCUKJST-UHFFFAOYSA-N atomic oxygen Chemical compound [O] QVGXLLKOCUKJST-UHFFFAOYSA-N 0.000 claims 1
- HONIICLYMWZJFZ-UHFFFAOYSA-N azetidine Chemical compound C1CNC1 HONIICLYMWZJFZ-UHFFFAOYSA-N 0.000 claims 1
- 201000011510 cancer Diseases 0.000 claims 1
- 230000006378 damage Effects 0.000 claims 1
- 239000003085 diluting agent Substances 0.000 claims 1
- WJJMNDUMQPNECX-UHFFFAOYSA-N dipicolinic acid Chemical group OC(=O)C1=CC=CC(C(O)=O)=N1 WJJMNDUMQPNECX-UHFFFAOYSA-N 0.000 claims 1
- 239000003814 drug Substances 0.000 claims 1
- 206010015037 epilepsy Diseases 0.000 claims 1
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims 1
- 208000030533 eye disease Diseases 0.000 claims 1
- 210000001035 gastrointestinal tract Anatomy 0.000 claims 1
- 125000001072 heteroaryl group Chemical group 0.000 claims 1
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims 1
- 125000004029 hydroxymethyl group Chemical group [H]OC([H])([H])* 0.000 claims 1
- 230000004054 inflammatory process Effects 0.000 claims 1
- 208000014674 injury Diseases 0.000 claims 1
- 230000001404 mediated effect Effects 0.000 claims 1
- 238000000034 method Methods 0.000 claims 1
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 1
- 230000004770 neurodegeneration Effects 0.000 claims 1
- 208000015122 neurodegenerative disease Diseases 0.000 claims 1
- 230000003959 neuroinflammation Effects 0.000 claims 1
- 201000001119 neuropathy Diseases 0.000 claims 1
- 230000007823 neuropathy Effects 0.000 claims 1
- 229910052757 nitrogen Inorganic materials 0.000 claims 1
- AQNQGBUEVCAVML-UHFFFAOYSA-N oxazepane Chemical compound C1CCNOCC1 AQNQGBUEVCAVML-UHFFFAOYSA-N 0.000 claims 1
- 229910052760 oxygen Inorganic materials 0.000 claims 1
- 239000001301 oxygen Substances 0.000 claims 1
- 208000033808 peripheral neuropathy Diseases 0.000 claims 1
- 239000008194 pharmaceutical composition Substances 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
- 230000002265 prevention Effects 0.000 claims 1
- 230000002062 proliferating effect Effects 0.000 claims 1
- 125000001436 propyl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])[H] 0.000 claims 1
- 208000020016 psychiatric disease Diseases 0.000 claims 1
- 125000000246 pyrimidin-2-yl group Chemical group [H]C1=NC(*)=NC([H])=C1[H] 0.000 claims 1
- 239000000126 substance Substances 0.000 claims 1
- 229910052717 sulfur Inorganic materials 0.000 claims 1
- 239000011593 sulfur Substances 0.000 claims 1
- 208000024891 symptom Diseases 0.000 claims 1
- 125000000999 tert-butyl group Chemical group [H]C([H])([H])C(*)(C([H])([H])[H])C([H])([H])[H] 0.000 claims 1
- 210000002229 urogenital system Anatomy 0.000 claims 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP14154038.5 | 2014-02-05 | ||
| EP14154038.5A EP2905282A1 (en) | 2014-02-05 | 2014-02-05 | Substituted thiazole or oxazole as P2X7 receptor antagonists |
| PCT/EP2015/052316 WO2015118019A1 (en) | 2014-02-05 | 2015-02-04 | Substituted thiazole or oxazole p2x7 receptor antagonists |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2017508733A JP2017508733A (ja) | 2017-03-30 |
| JP2017508733A5 true JP2017508733A5 (OSRAM) | 2021-01-21 |
| JP6858560B2 JP6858560B2 (ja) | 2021-04-14 |
Family
ID=50033404
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2016550583A Active JP6858560B2 (ja) | 2014-02-05 | 2015-02-04 | 置換チアゾールまたはオキサゾールｐ２ｘ７受容体拮抗薬 |
Country Status (19)
| Country | Link |
|---|---|
| US (2) | US9718812B2 (OSRAM) |
| EP (2) | EP2905282A1 (OSRAM) |
| JP (1) | JP6858560B2 (OSRAM) |
| CN (1) | CN106103432B (OSRAM) |
| CA (1) | CA2938703C (OSRAM) |
| CY (1) | CY1120295T1 (OSRAM) |
| DK (1) | DK3102573T3 (OSRAM) |
| ES (1) | ES2670093T3 (OSRAM) |
| HR (1) | HRP20180973T1 (OSRAM) |
| HU (1) | HUE037545T2 (OSRAM) |
| IL (1) | IL247081B (OSRAM) |
| LT (1) | LT3102573T (OSRAM) |
| PL (1) | PL3102573T3 (OSRAM) |
| PT (1) | PT3102573T (OSRAM) |
| RS (1) | RS57415B1 (OSRAM) |
| RU (1) | RU2701858C1 (OSRAM) |
| SI (1) | SI3102573T1 (OSRAM) |
| TR (1) | TR201809769T4 (OSRAM) |
| WO (1) | WO2015118019A1 (OSRAM) |
Families Citing this family (10)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP2905282A1 (en) * | 2014-02-05 | 2015-08-12 | AXXAM S.p.A. | Substituted thiazole or oxazole as P2X7 receptor antagonists |
| EP3290417A1 (en) | 2016-08-31 | 2018-03-07 | AXXAM S.p.A. | 2-chloro-n-[2-(1,3-thiazol-5-yl)ethyl]-5-(5-fluoropyrimidin-2-yl)-benzamides and their use as p2x7 receptor antagonists |
| EP3290416A1 (en) | 2016-08-31 | 2018-03-07 | AXXAM S.p.A. | Substituted n-[2-(4-phenoxypiperidin-1-yl)-2-(1,3-thiazol-5-yl)ethyl]benzamide and n-[2-(4-benzyloxypiperidin-1-yl)-2-(1,3-thiazol-5-yl)ethyl]benzamide derivatives and their use as p2x7 receptor antagonist |
| CN106562947A (zh) * | 2016-11-03 | 2017-04-19 | 南昌大学 | 亮蓝g在制备人类免疫缺陷病毒糖蛋白120诱导神经病理痛药物中的应用 |
| CN111377867B (zh) * | 2018-12-28 | 2022-09-06 | 南京药石科技股份有限公司 | 一种合成2-(1-烷基-1h-吡唑-4-基)吗啉的中间体及其制备方法和应用 |
| EP3936192B1 (en) | 2019-03-06 | 2025-04-09 | Daiichi Sankyo Company, Limited | Pyrrolopyrazole derivative |
| MA55805A (fr) | 2019-05-03 | 2022-03-09 | Flagship Pioneering Innovations V Inc | Métodes de modulation de l'activité immunitaire |
| EP4015039A1 (en) * | 2020-12-18 | 2022-06-22 | AXXAM S.p.A. | Heterocyclic derivatives as p2x7 receptor antagonists |
| CN113968806A (zh) * | 2021-10-12 | 2022-01-25 | 北京科技大学 | 一种非对称硫代酰胺类萃取剂及其合成方法 |
| CN115305282A (zh) * | 2022-08-04 | 2022-11-08 | 烟台毓璜顶医院 | 一种用于AR-induced OD诊断和预后判别的靶点及治疗方法 |
Family Cites Families (15)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2003128639A (ja) * | 2001-10-25 | 2003-05-08 | Sankyo Co Ltd | ベンツアミド誘導体 |
| DE10237722A1 (de) * | 2002-08-17 | 2004-08-19 | Aventis Pharma Deutschland Gmbh | Indol- oder Benzimidazolderivate zur Modulation der IKappaB-Kinase |
| JP4731468B2 (ja) * | 2003-05-12 | 2011-07-27 | ファイザー・プロダクツ・インク | Ｐ２ｘ７受容体のベンズアミド阻害剤 |
| BRPI0718714B8 (pt) * | 2006-11-09 | 2021-05-25 | Hoffmann La Roche | arilamidas substituídas por tiazol e oxazol, seu uso e composição farmacêutica que as compreende |
| ITMC20070152A1 (it) * | 2007-07-26 | 2009-01-27 | Faggiolati Pumps Spa | Miscelatore sommerso in particolare miscelatore sommerso per vasche di trattamento delle acque reflue. |
| US8461185B2 (en) * | 2007-10-31 | 2013-06-11 | Merck Sharp & Dohme Corp. | P2X3 receptor antagonists for treatment of pain |
| WO2009108551A2 (en) | 2008-02-25 | 2009-09-03 | H. Lundbeck A/S | Heteroaryl amide analogues |
| EP2262766B1 (en) * | 2008-02-29 | 2015-11-11 | Evotec AG | Amide compounds, compositions and uses thereof |
| ES2376092T3 (es) | 2008-04-22 | 2012-03-08 | Janssen Pharmaceutica, N.V. | Antagonistas de p2x7 sustituidos con quinolina o isoquinolina. |
| CA2741666C (en) * | 2008-10-31 | 2017-04-11 | Merck Sharp & Dohme Corp. | P2x3, receptor antagonists for treatment of pain |
| EP2410858B1 (en) * | 2009-03-23 | 2016-09-07 | Merck Sharp & Dohme Corp. | P2x3 receptor antagonists for treatment of pain |
| US9238647B2 (en) * | 2009-03-23 | 2016-01-19 | Merck Sharp & Dohme Corp. | P2X3 receptor antagonists for treatment of pain |
| AU2010229144B2 (en) * | 2009-03-23 | 2012-07-12 | Merck Sharp & Dohme Corp. | P2X3, receptor antagonists for treatment of pain |
| EP2931717B1 (en) * | 2012-12-12 | 2016-12-07 | Actelion Pharmaceuticals Ltd. | Indole carboxamide derivatives as p2x7 receptor antagonists |
| EP2905282A1 (en) * | 2014-02-05 | 2015-08-12 | AXXAM S.p.A. | Substituted thiazole or oxazole as P2X7 receptor antagonists |
-
2014
- 2014-02-05 EP EP14154038.5A patent/EP2905282A1/en not_active Withdrawn
-
2015
- 2015-02-04 SI SI201530274T patent/SI3102573T1/en unknown
- 2015-02-04 CA CA2938703A patent/CA2938703C/en active Active
- 2015-02-04 PL PL15705523T patent/PL3102573T3/pl unknown
- 2015-02-04 JP JP2016550583A patent/JP6858560B2/ja active Active
- 2015-02-04 EP EP15705523.7A patent/EP3102573B1/en active Active
- 2015-02-04 WO PCT/EP2015/052316 patent/WO2015118019A1/en not_active Ceased
- 2015-02-04 US US15/115,963 patent/US9718812B2/en active Active
- 2015-02-04 RS RS20180763A patent/RS57415B1/sr unknown
- 2015-02-04 HR HRP20180973TT patent/HRP20180973T1/hr unknown
- 2015-02-04 LT LTEP15705523.7T patent/LT3102573T/lt unknown
- 2015-02-04 DK DK15705523.7T patent/DK3102573T3/en active
- 2015-02-04 TR TR2018/09769T patent/TR201809769T4/tr unknown
- 2015-02-04 CN CN201580007048.8A patent/CN106103432B/zh active Active
- 2015-02-04 RU RU2016131689A patent/RU2701858C1/ru active
- 2015-02-04 HU HUE15705523A patent/HUE037545T2/hu unknown
- 2015-02-04 PT PT157055237T patent/PT3102573T/pt unknown
- 2015-02-04 ES ES15705523.7T patent/ES2670093T3/es active Active
-
2016
- 2016-08-03 IL IL24708116A patent/IL247081B/en active IP Right Grant
-
2017
- 2017-06-18 US US15/626,138 patent/US10167281B2/en active Active
-
2018
- 2018-05-31 CY CY20181100582T patent/CY1120295T1/el unknown
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