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 (https=) | 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 (26)
| Country | Link |
|---|---|
| US (2) | US10716788B2 (https=) |
| EP (2) | EP4295910A3 (https=) |
| JP (1) | JP6891173B2 (https=) |
| KR (1) | KR102780243B1 (https=) |
| CN (1) | CN108884076B (https=) |
| AU (1) | AU2016357735B2 (https=) |
| BR (1) | BR112018007517B1 (https=) |
| CL (1) | CL2018001252A1 (https=) |
| DK (1) | DK3377484T3 (https=) |
| ES (1) | ES2964946T3 (https=) |
| FI (1) | FI3377484T3 (https=) |
| HR (1) | HRP20231547T1 (https=) |
| HU (1) | HUE064244T2 (https=) |
| IL (1) | IL258978B (https=) |
| LT (1) | LT3377484T (https=) |
| MX (1) | MX386146B (https=) |
| MY (1) | MY199473A (https=) |
| NZ (1) | NZ741294A (https=) |
| PH (1) | PH12018500736A1 (https=) |
| PL (1) | PL3377484T3 (https=) |
| PT (1) | PT3377484T (https=) |
| RS (1) | RS64908B1 (https=) |
| SI (1) | SI3377484T1 (https=) |
| UA (1) | UA123159C2 (https=) |
| WO (1) | WO2017087445A1 (https=) |
| ZA (1) | ZA201802348B (https=) |
Families Citing this family (13)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| PL3371165T3 (pl) * | 2015-11-04 | 2022-05-02 | Merck Patent Gmbh | Inhibitor btk do zastosowania w terapii rakowej |
| KR102780243B1 (ko) * | 2015-11-17 | 2025-03-14 | 메르크 파텐트 게엠베하 | Btk 억제 활성을 갖는 피리미딘 및 피리딘 화합물을 사용하여 다발성 경화증을 치료하는 방법 |
| CN112313214A (zh) * | 2018-06-19 | 2021-02-02 | 默克专利有限公司 | 1-(4-{[6-氨基-5-(4-苯氧基-苯基)-嘧啶-4-基氨基]-甲基}-4-氟代-哌啶-1-基)-丙烯酮及其盐形式的新晶体形式以及获得方法 |
| MX2021000094A (es) * | 2018-07-20 | 2021-03-25 | Merck Patent Gmbh | Compuesto de amino-pirimidina sustituido para usarse en un metodo para tratamiento y prevencion de esclerosis multiple. |
| EP4093397A1 (en) | 2020-01-20 | 2022-11-30 | Genzyme Corporation | Therapeutic tyrosine kinase inhibitors for relapsing multiple sclerosis (rms) |
| 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 |
| MX2023006418A (es) * | 2020-12-02 | 2023-06-13 | Telios Pharma Inc | Metodos y composiciones para el tratamiento de una afeccion oftalmica. |
| AU2021398051A1 (en) | 2020-12-10 | 2023-07-27 | Principia Biopharma Inc. | Crystal form of tolebrutinib, preparation method therefor and use thereof |
| US11866421B2 (en) | 2021-05-31 | 2024-01-09 | Epigen Biosciences, Inc. | Pyrimidine and pyridine amine compounds and usage thereof in disease treatment |
| CN119744171A (zh) | 2022-06-24 | 2025-04-01 | 默克专利股份公司 | 自身免疫病和炎性疾病的治疗方案 |
| 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 |
| US12414950B1 (en) * | 2024-05-21 | 2025-09-16 | Telios Pharma Inc. | Methods of treating indolent systemic mastocytosis |
Family Cites Families (17)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| AR038955A1 (es) | 1996-12-05 | 2005-02-02 | Amgen Inc | Compuestos de pirimidinona y piridona sustituidos y metodos para su uso |
| TWI372624B (en) | 2004-03-30 | 2012-09-21 | Vertex Pharma | Azaindoles useful as inhibitors of jak and other protein kinases |
| GB0512844D0 (en) | 2005-06-23 | 2005-08-03 | Novartis Ag | Organic compounds |
| BRPI0622054B8 (pt) | 2006-09-22 | 2021-05-25 | Oxford Amherst Llc | composto e composição farmacêutica |
| US20100311736A1 (en) | 2007-10-22 | 2010-12-09 | Glaxosmithkline Llc | Pyridosulfonamide derivatives as p13 kinase inhibitors |
| EP2475667A1 (en) | 2009-09-10 | 2012-07-18 | 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 |
| JP6178861B2 (ja) * | 2012-11-02 | 2017-08-09 | ファイザー・インク | ブルトン型チロシンキナーゼ阻害剤 |
| 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 |
| JP6272832B2 (ja) | 2013-04-04 | 2018-01-31 | 武田薬品工業株式会社 | 複素環化合物 |
| JP6509838B2 (ja) * | 2013-06-26 | 2019-05-08 | アッヴィ・インコーポレイテッド | Ｂｔｋ阻害薬としての一級カルボキサミド類 |
| CA2918242C (en) * | 2013-07-31 | 2022-06-21 | Merck Patent Gmbh | Pyridines, pyrimidines, and pyrazines, as btk inhibitors and uses thereof |
| US9657007B2 (en) * | 2013-09-22 | 2017-05-23 | Calitor Sciences, Llc | Substituted aminopyrimidine compounds and methods of use |
| PL3371165T3 (pl) * | 2015-11-04 | 2022-05-02 | Merck Patent Gmbh | Inhibitor btk do zastosowania w terapii rakowej |
| KR102780243B1 (ko) * | 2015-11-17 | 2025-03-14 | 메르크 파텐트 게엠베하 | Btk 억제 활성을 갖는 피리미딘 및 피리딘 화합물을 사용하여 다발성 경화증을 치료하는 방법 |
-
2016
- 2016-11-16 KR KR1020187014258A patent/KR102780243B1/ko active Active
- 2016-11-16 DK DK16805251.2T patent/DK3377484T3/da active
- 2016-11-16 WO PCT/US2016/062154 patent/WO2017087445A1/en not_active Ceased
- 2016-11-16 HU HUE16805251A patent/HUE064244T2/hu unknown
- 2016-11-16 CN CN201680078780.9A patent/CN108884076B/zh active Active
- 2016-11-16 JP JP2018525702A patent/JP6891173B2/ja active Active
- 2016-11-16 RS RS20231155A patent/RS64908B1/sr unknown
- 2016-11-16 BR BR112018007517-5A patent/BR112018007517B1/pt active IP Right Grant
- 2016-11-16 ES ES16805251T patent/ES2964946T3/es active Active
- 2016-11-16 SI SI201631768T patent/SI3377484T1/sl unknown
- 2016-11-16 PL PL16805251.2T patent/PL3377484T3/pl unknown
- 2016-11-16 LT LTEPPCT/US2016/062154T patent/LT3377484T/lt unknown
- 2016-11-16 EP EP23195454.6A patent/EP4295910A3/en active Pending
- 2016-11-16 FI FIEP16805251.2T patent/FI3377484T3/fi active
- 2016-11-16 EP EP16805251.2A patent/EP3377484B1/en active Active
- 2016-11-16 NZ NZ741294A patent/NZ741294A/en unknown
- 2016-11-16 US US15/352,657 patent/US10716788B2/en active Active
- 2016-11-16 AU AU2016357735A patent/AU2016357735B2/en active Active
- 2016-11-16 UA UAA201806687A patent/UA123159C2/uk unknown
- 2016-11-16 MX MX2018005463A patent/MX386146B/es unknown
- 2016-11-16 PT PT168052512T patent/PT3377484T/pt unknown
- 2016-11-16 HR HRP20231547TT patent/HRP20231547T1/hr unknown
- 2016-11-16 MY MYPI2018701467A patent/MY199473A/en 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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