JP2018538264A5 - - Google Patents
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- Publication number
- JP2018538264A5 JP2018538264A5 JP2018525702A JP2018525702A JP2018538264A5 JP 2018538264 A5 JP2018538264 A5 JP 2018538264A5 JP 2018525702 A JP2018525702 A JP 2018525702A JP 2018525702 A JP2018525702 A JP 2018525702A JP 2018538264 A5 JP2018538264 A5 JP 2018538264A5
- Authority
- JP
- Japan
- Prior art keywords
- het
- hal
- unsubstituted
- atoms
- mono
- 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
- -1 tri-substituted phenyl Chemical group 0.000 claims 35
- 239000008194 pharmaceutical composition Substances 0.000 claims 15
- 125000004432 carbon atom Chemical group C* 0.000 claims 10
- 125000006297 carbonyl amino group Chemical group [H]N([*:2])C([*:1])=O 0.000 claims 10
- IJGRMHOSHXDMSA-UHFFFAOYSA-N Atomic nitrogen Chemical compound N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims 9
- 229910052760 oxygen Inorganic materials 0.000 claims 9
- 125000002347 octyl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])[H] 0.000 claims 8
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 8
- 125000003386 piperidinyl group Chemical group 0.000 claims 8
- QVGXLLKOCUKJST-UHFFFAOYSA-N atomic oxygen Chemical compound [O] QVGXLLKOCUKJST-UHFFFAOYSA-N 0.000 claims 7
- 150000001875 compounds Chemical class 0.000 claims 7
- 125000005842 heteroatom Chemical group 0.000 claims 7
- 125000002757 morpholinyl group Chemical group 0.000 claims 7
- 229910052757 nitrogen Inorganic materials 0.000 claims 7
- 239000001301 oxygen Substances 0.000 claims 7
- 125000004430 oxygen atom Chemical group O* 0.000 claims 7
- 125000004193 piperazinyl group Chemical group 0.000 claims 7
- 125000004076 pyridyl group Chemical group 0.000 claims 7
- 125000000719 pyrrolidinyl group Chemical group 0.000 claims 7
- 125000000217 alkyl group Chemical group 0.000 claims 6
- 125000003725 azepanyl group Chemical group 0.000 claims 6
- 125000002393 azetidinyl group Chemical group 0.000 claims 6
- 125000004925 dihydropyridyl group Chemical group N1(CC=CC=C1)* 0.000 claims 6
- 125000000623 heterocyclic group Chemical group 0.000 claims 6
- 125000002632 imidazolidinyl group Chemical group 0.000 claims 6
- 125000001715 oxadiazolyl group Chemical group 0.000 claims 6
- 125000003226 pyrazolyl group Chemical group 0.000 claims 6
- 125000000714 pyrimidinyl group Chemical group 0.000 claims 6
- 229920006395 saturated elastomer Polymers 0.000 claims 6
- 125000005942 tetrahydropyridyl group Chemical group 0.000 claims 6
- 125000001544 thienyl group Chemical group 0.000 claims 6
- 125000002619 bicyclic group Chemical group 0.000 claims 5
- 125000005879 dioxolanyl group Chemical group 0.000 claims 5
- 229910052731 fluorine Inorganic materials 0.000 claims 5
- 125000002541 furyl group Chemical group 0.000 claims 5
- 125000002883 imidazolyl group Chemical group 0.000 claims 5
- 125000002950 monocyclic group Chemical group 0.000 claims 5
- 125000000168 pyrrolyl group Chemical group 0.000 claims 5
- 125000003718 tetrahydrofuranyl group Chemical group 0.000 claims 5
- 125000005958 tetrahydrothienyl group Chemical group 0.000 claims 5
- 125000005052 dihydropyrazolyl group Chemical group N1(NCC=C1)* 0.000 claims 4
- 125000005054 dihydropyrrolyl group Chemical group [H]C1=C([H])C([H])([H])C([H])([H])N1* 0.000 claims 4
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims 4
- 125000001786 isothiazolyl group Chemical group 0.000 claims 4
- 125000000842 isoxazolyl group Chemical group 0.000 claims 4
- 125000001624 naphthyl group Chemical group 0.000 claims 4
- 125000004433 nitrogen atom Chemical group N* 0.000 claims 4
- 125000002971 oxazolyl group Chemical group 0.000 claims 4
- 125000003373 pyrazinyl group Chemical group 0.000 claims 4
- 125000002098 pyridazinyl group Chemical group 0.000 claims 4
- 125000004434 sulfur atom Chemical group 0.000 claims 4
- 125000003831 tetrazolyl group Chemical group 0.000 claims 4
- 125000001113 thiadiazolyl group Chemical group 0.000 claims 4
- 125000000335 thiazolyl group Chemical group 0.000 claims 4
- 125000001425 triazolyl group Chemical group 0.000 claims 4
- DHXVGJBLRPWPCS-UHFFFAOYSA-N Tetrahydropyran Chemical compound C1CCOCC1 DHXVGJBLRPWPCS-UHFFFAOYSA-N 0.000 claims 3
- 125000004603 benzisoxazolyl group Chemical group O1N=C(C2=C1C=CC=C2)* 0.000 claims 3
- 229910052794 bromium Inorganic materials 0.000 claims 3
- 229910052801 chlorine Inorganic materials 0.000 claims 3
- 229910052739 hydrogen Inorganic materials 0.000 claims 3
- 229910052740 iodine Inorganic materials 0.000 claims 3
- 208000007400 Relapsing-Remitting Multiple Sclerosis Diseases 0.000 claims 2
- 125000002947 alkylene group Chemical group 0.000 claims 2
- 125000006615 aromatic heterocyclic group Chemical group 0.000 claims 2
- 125000003785 benzimidazolyl group Chemical group N1=C(NC2=C1C=CC=C2)* 0.000 claims 2
- 125000005605 benzo group Chemical group 0.000 claims 2
- 125000003354 benzotriazolyl group Chemical group N1N=NC2=C1C=CC=C2* 0.000 claims 2
- 125000000723 dihydrobenzofuranyl group Chemical group O1C(CC2=C1C=CC=C2)* 0.000 claims 2
- 125000003453 indazolyl group Chemical group N1N=C(C2=C1C=CC=C2)* 0.000 claims 2
- 125000001041 indolyl group Chemical group 0.000 claims 2
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 2
- 206010063401 primary progressive multiple sclerosis Diseases 0.000 claims 2
- 230000000750 progressive effect Effects 0.000 claims 2
- 201000008628 secondary progressive multiple sclerosis Diseases 0.000 claims 2
- HGINCPLSRVDWNT-UHFFFAOYSA-N Acrolein Chemical compound C=CC=O HGINCPLSRVDWNT-UHFFFAOYSA-N 0.000 claims 1
- 239000004480 active ingredient Substances 0.000 claims 1
- 239000002671 adjuvant Substances 0.000 claims 1
- 125000003118 aryl group Chemical group 0.000 claims 1
- 125000004429 atom Chemical group 0.000 claims 1
- 125000001797 benzyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])* 0.000 claims 1
- 125000000753 cycloalkyl group Chemical group 0.000 claims 1
- ZZUFCTLCJUWOSV-UHFFFAOYSA-N furosemide Chemical compound C1=C(Cl)C(S(=O)(=O)N)=CC(C(O)=O)=C1NCC1=CC=CO1 ZZUFCTLCJUWOSV-UHFFFAOYSA-N 0.000 claims 1
- 229910052736 halogen Inorganic materials 0.000 claims 1
- 150000002367 halogens Chemical class 0.000 claims 1
- 125000001072 heteroaryl group Chemical group 0.000 claims 1
- 239000001257 hydrogen Substances 0.000 claims 1
- 125000005647 linker group Chemical group 0.000 claims 1
- 238000000034 method Methods 0.000 claims 1
- 239000000203 mixture Substances 0.000 claims 1
- 125000000896 monocarboxylic acid group Chemical group 0.000 claims 1
- 150000002825 nitriles Chemical class 0.000 claims 1
- QJGQUHMNIGDVPM-UHFFFAOYSA-N nitrogen group Chemical group [N] QJGQUHMNIGDVPM-UHFFFAOYSA-N 0.000 claims 1
- 239000000546 pharmaceutical excipient Substances 0.000 claims 1
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims 1
- 150000003839 salts Chemical class 0.000 claims 1
- 238000002560 therapeutic procedure Methods 0.000 claims 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201562256199P | 2015-11-17 | 2015-11-17 | |
| US62/256,199 | 2015-11-17 | ||
| PCT/US2016/062154 WO2017087445A1 (en) | 2015-11-17 | 2016-11-16 | Methods for treating multiple sclerosis using pyrimidine and pyridine compounds with btk inhibitory activity |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2018538264A JP2018538264A (ja) | 2018-12-27 |
| JP2018538264A5 true JP2018538264A5 (OSRAM) | 2019-12-26 |
| JP6891173B2 JP6891173B2 (ja) | 2021-06-18 |
Family
ID=57460611
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2018525702A Active JP6891173B2 (ja) | 2015-11-17 | 2016-11-16 | Ｂｔｋ阻害活性を有するピリミジン及びピリジン化合物を用いたｍｓの治療方法 |
Country Status (27)
| Country | Link |
|---|---|
| US (2) | US10716788B2 (OSRAM) |
| EP (2) | EP3377484B1 (OSRAM) |
| JP (1) | JP6891173B2 (OSRAM) |
| KR (1) | KR102780243B1 (OSRAM) |
| CN (1) | CN108884076B (OSRAM) |
| AU (1) | AU2016357735B2 (OSRAM) |
| BR (1) | BR112018007517B1 (OSRAM) |
| CA (1) | CA3002224A1 (OSRAM) |
| CL (1) | CL2018001252A1 (OSRAM) |
| DK (1) | DK3377484T3 (OSRAM) |
| ES (1) | ES2964946T3 (OSRAM) |
| FI (1) | FI3377484T3 (OSRAM) |
| HR (1) | HRP20231547T1 (OSRAM) |
| HU (1) | HUE064244T2 (OSRAM) |
| IL (1) | IL258978B (OSRAM) |
| LT (1) | LT3377484T (OSRAM) |
| MX (1) | MX386146B (OSRAM) |
| MY (1) | MY199473A (OSRAM) |
| NZ (1) | NZ741294A (OSRAM) |
| PH (1) | PH12018500736A1 (OSRAM) |
| PL (1) | PL3377484T3 (OSRAM) |
| PT (1) | PT3377484T (OSRAM) |
| RS (1) | RS64908B1 (OSRAM) |
| SI (1) | SI3377484T1 (OSRAM) |
| UA (1) | UA123159C2 (OSRAM) |
| WO (1) | WO2017087445A1 (OSRAM) |
| ZA (1) | ZA201802348B (OSRAM) |
Families Citing this family (12)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| TWI858413B (zh) * | 2015-11-04 | 2024-10-11 | 德商默克專利有限公司 | 具有ｂｔｋ抑制活性之嘧啶及吡啶化合物之用途 |
| US10716788B2 (en) * | 2015-11-17 | 2020-07-21 | Merck Patent Gmbh | Methods for treating MS using pyrimidine and pyridine compounds with BTK inhibitory activity |
| WO2019243223A1 (en) * | 2018-06-19 | 2019-12-26 | Merck Patent Gmbh | Novel crystalline forms of 1-(4-{[6-amino-5-(4-phenoxy-phenyl)-pyrimidin-4-ylamino]-methyl}-4-fluoro-piperidin-1-yl)-propenone, salt forms thereof, and processes to obtain |
| JP7724151B2 (ja) * | 2018-07-20 | 2025-08-15 | メルク パテント ゲゼルシャフト ミット ベシュレンクテル ハフツング | 多発性硬化症の治療及び予防方法における使用のための置換されたアミノ－ピリミジン化合物 |
| MX2022008875A (es) | 2020-01-20 | 2022-08-11 | Genzyme Corp | Inhibidores terapeuticos de tirosina quinasa para esclerosis multiple recidivante (emr). |
| CN112250666B (zh) * | 2020-10-09 | 2022-01-14 | 广东东阳光药业有限公司 | 取代的嘧啶类化合物及其用途 |
| CA3200332A1 (en) * | 2020-12-02 | 2022-06-09 | Telios Pharma, Inc. | Methods and compositions for treating an ophthalmic condition |
| CA3201936A1 (en) | 2020-12-10 | 2022-06-16 | Minhua Chen | Crystal form of tolebrutinib and preparation method thereof |
| US11866421B2 (en) | 2021-05-31 | 2024-01-09 | Epigen Biosciences, Inc. | Pyrimidine and pyridine amine compounds and usage thereof in disease treatment |
| AU2023286839A1 (en) | 2022-06-24 | 2025-02-13 | Merck Patent Gmbh | Treatment regimen for autoimmune diseases and inflammatory diseases |
| CN117986236B (zh) * | 2022-11-07 | 2024-12-31 | 天津征程医药科技有限公司 | 氘代的嘧啶衍生物以及包含该化合物的药物组合物 |
| WO2025096900A1 (en) * | 2023-11-03 | 2025-05-08 | Board Of Regents, The University Of Texas System | Synthetic network materials and methods of making and use thereof |
Family Cites Families (17)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2002514195A (ja) * | 1996-12-05 | 2002-05-14 | アムジエン・インコーポレーテツド | 置換ピリミジン化合物およびそれの使用 |
| WO2005095400A1 (en) | 2004-03-30 | 2005-10-13 | Vertex Pharmaceuticals Incorporated | Azaindoles useful as inhibitors of jak and other protein kinases |
| GB0512844D0 (en) * | 2005-06-23 | 2005-08-03 | Novartis Ag | Organic compounds |
| EP2526934B1 (en) * | 2006-09-22 | 2015-12-09 | Pharmacyclics LLC | Inhibitors of bruton's tyrosine kinase |
| WO2009055418A1 (en) * | 2007-10-22 | 2009-04-30 | Smithkline Beecham Corporation | Pyridosulfonamide derivatives as pi3 kinase inhibitors |
| CA2773182A1 (en) | 2009-09-10 | 2011-03-17 | F. Hoffmann-La Roche Ag | Inhibitors of jak |
| KR101301533B1 (ko) | 2010-02-09 | 2013-09-04 | 한미사이언스 주식회사 | 암세포 성장 억제 효과를 갖는 신규 피리미딘 유도체 |
| KR20180084153A (ko) * | 2011-06-10 | 2018-07-24 | 메르크 파텐트 게엠베하 | Btk 억제 활성을 갖는 피리미딘 및 피리딘 화합물의 조성물 및 제조방법 |
| TW201414734A (zh) * | 2012-07-10 | 2014-04-16 | Takeda Pharmaceutical | 氮雜吲哚衍生物 |
| WO2014068527A1 (en) * | 2012-11-02 | 2014-05-08 | Pfizer Inc. | Bruton's tyrosine kinase inhibitors |
| WO2014093230A2 (en) * | 2012-12-10 | 2014-06-19 | Merck Patent Gmbh | Compositions and methods for the production of pyrimidine and pyridine compounds with btk inhibitory activity |
| WO2014163161A1 (ja) * | 2013-04-04 | 2014-10-09 | 武田薬品工業株式会社 | 複素環化合物 |
| NZ754039A (en) * | 2013-06-26 | 2021-06-25 | Abbvie Inc | Primary carboxamides as btk inhibitors |
| RU2712220C2 (ru) * | 2013-07-31 | 2020-01-27 | Мерк Патент Гмбх | Пиридины, пиримидины и пиразины в качестве ингибиторов тирозинкиназы брутона и их применение |
| CA2918938C (en) | 2013-09-22 | 2021-05-18 | Calitor Sciences, Llc | Substituted aminopyrimidine compounds and methods of use |
| TWI858413B (zh) * | 2015-11-04 | 2024-10-11 | 德商默克專利有限公司 | 具有ｂｔｋ抑制活性之嘧啶及吡啶化合物之用途 |
| US10716788B2 (en) * | 2015-11-17 | 2020-07-21 | Merck Patent Gmbh | Methods for treating MS using pyrimidine and pyridine compounds with BTK inhibitory activity |
-
2016
- 2016-11-16 US US15/352,657 patent/US10716788B2/en active Active
- 2016-11-16 WO PCT/US2016/062154 patent/WO2017087445A1/en not_active Ceased
- 2016-11-16 RS RS20231155A patent/RS64908B1/sr unknown
- 2016-11-16 FI FIEP16805251.2T patent/FI3377484T3/fi active
- 2016-11-16 KR KR1020187014258A patent/KR102780243B1/ko active Active
- 2016-11-16 MX MX2018005463A patent/MX386146B/es unknown
- 2016-11-16 JP JP2018525702A patent/JP6891173B2/ja active Active
- 2016-11-16 CN CN201680078780.9A patent/CN108884076B/zh active Active
- 2016-11-16 NZ NZ741294A patent/NZ741294A/en unknown
- 2016-11-16 SI SI201631768T patent/SI3377484T1/sl unknown
- 2016-11-16 EP EP16805251.2A patent/EP3377484B1/en active Active
- 2016-11-16 MY MYPI2018701467A patent/MY199473A/en unknown
- 2016-11-16 DK DK16805251.2T patent/DK3377484T3/da active
- 2016-11-16 BR BR112018007517-5A patent/BR112018007517B1/pt active IP Right Grant
- 2016-11-16 LT LTEPPCT/US2016/062154T patent/LT3377484T/lt unknown
- 2016-11-16 UA UAA201806687A patent/UA123159C2/uk unknown
- 2016-11-16 HR HRP20231547TT patent/HRP20231547T1/hr unknown
- 2016-11-16 EP EP23195454.6A patent/EP4295910A3/en active Pending
- 2016-11-16 PL PL16805251.2T patent/PL3377484T3/pl unknown
- 2016-11-16 AU AU2016357735A patent/AU2016357735B2/en active Active
- 2016-11-16 ES ES16805251T patent/ES2964946T3/es active Active
- 2016-11-16 PT PT168052512T patent/PT3377484T/pt unknown
- 2016-11-16 CA CA3002224A patent/CA3002224A1/en active Pending
- 2016-11-16 HU HUE16805251A patent/HUE064244T2/hu unknown
-
2018
- 2018-04-03 PH PH12018500736A patent/PH12018500736A1/en unknown
- 2018-04-10 ZA ZA2018/02348A patent/ZA201802348B/en unknown
- 2018-04-26 IL IL258978A patent/IL258978B/en active IP Right Grant
- 2018-05-09 CL CL2018001252A patent/CL2018001252A1/es unknown
-
2020
- 2020-06-08 US US16/946,145 patent/US20200316068A1/en not_active Abandoned
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