JP2019519581A5 - - Google Patents
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- JP2019519581A5 JP2019519581A5 JP2018568426A JP2018568426A JP2019519581A5 JP 2019519581 A5 JP2019519581 A5 JP 2019519581A5 JP 2018568426 A JP2018568426 A JP 2018568426A JP 2018568426 A JP2018568426 A JP 2018568426A JP 2019519581 A5 JP2019519581 A5 JP 2019519581A5
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- JP
- Japan
- Prior art keywords
- solid oral
- modified release
- release solid
- oral formulation
- compound
- 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.)
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- 239000000203 mixture Substances 0.000 claims 44
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- 150000003839 salts Chemical class 0.000 claims 11
- 239000002702 enteric coating Substances 0.000 claims 7
- 238000009505 enteric coating Methods 0.000 claims 7
- 239000010410 layer Substances 0.000 claims 7
- 239000006186 oral dosage form Substances 0.000 claims 6
- 239000004372 Polyvinyl alcohol Substances 0.000 claims 5
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- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 5
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- UFVKGYZPFZQRLF-UHFFFAOYSA-N hydroxypropyl methyl cellulose Chemical compound OC1C(O)C(OC)OC(CO)C1OC1C(O)C(O)C(OC2C(C(O)C(OC3C(C(O)C(O)C(CO)O3)O)C(CO)O2)O)C(CO)O1 UFVKGYZPFZQRLF-UHFFFAOYSA-N 0.000 claims 5
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- 102000001714 Agammaglobulinaemia Tyrosine Kinase Human genes 0.000 claims 4
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- ISBHMJZRKAFTGE-ONEGZZNKSA-N (e)-pent-2-enenitrile Chemical compound CC\C=C\C#N ISBHMJZRKAFTGE-ONEGZZNKSA-N 0.000 claims 2
- SMZOUWXMTYCWNB-UHFFFAOYSA-N 2-(2-methoxy-5-methylphenyl)ethanamine Chemical compound COC1=CC=C(C)C=C1CCN SMZOUWXMTYCWNB-UHFFFAOYSA-N 0.000 claims 2
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- CERQOIWHTDAKMF-UHFFFAOYSA-N Methacrylic acid Chemical compound CC(=C)C(O)=O CERQOIWHTDAKMF-UHFFFAOYSA-N 0.000 claims 2
- VVQNEPGJFQJSBK-UHFFFAOYSA-N Methyl methacrylate Chemical group COC(=O)C(C)=C VVQNEPGJFQJSBK-UHFFFAOYSA-N 0.000 claims 2
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- MVPICKVDHDWCJQ-UHFFFAOYSA-N ethyl 3-pyrrolidin-1-ylpropanoate Chemical group CCOC(=O)CCN1CCCC1 MVPICKVDHDWCJQ-UHFFFAOYSA-N 0.000 claims 2
- 239000000945 filler Substances 0.000 claims 2
- 229920003132 hydroxypropyl methylcellulose phthalate Polymers 0.000 claims 2
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- 125000004194 piperazin-1-yl group Chemical group [H]N1C([H])([H])C([H])([H])N(*)C([H])([H])C1([H])[H] 0.000 claims 2
- 239000004014 plasticizer Substances 0.000 claims 2
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- 229940045902 sodium stearyl fumarate Drugs 0.000 claims 2
- 201000000596 systemic lupus erythematosus Diseases 0.000 claims 2
- JNYAEWCLZODPBN-JGWLITMVSA-N (2r,3r,4s)-2-[(1r)-1,2-dihydroxyethyl]oxolane-3,4-diol Polymers OC[C@@H](O)[C@H]1OC[C@H](O)[C@H]1O JNYAEWCLZODPBN-JGWLITMVSA-N 0.000 claims 1
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- WRIDQFICGBMAFQ-UHFFFAOYSA-N (E)-8-Octadecenoic acid Natural products CCCCCCCCCC=CCCCCCCC(O)=O WRIDQFICGBMAFQ-UHFFFAOYSA-N 0.000 claims 1
- JNYAEWCLZODPBN-UHFFFAOYSA-N 2-(1,2-dihydroxyethyl)oxolane-3,4-diol Polymers OCC(O)C1OCC(O)C1O JNYAEWCLZODPBN-UHFFFAOYSA-N 0.000 claims 1
- LCFFREMLXLZNHE-RUZDIDTESA-N 2-[(3R)-3-[4-amino-3-(2-fluoro-4-phenoxyphenyl)pyrazolo[3,4-d]pyrimidin-1-yl]piperidine-1-carbonyl]-4-methyl-4-[4-(oxetan-3-yl)piperazin-1-yl]pent-2-enenitrile Chemical compound CC(C)(C=C(C#N)C(=O)N1CCC[C@H](C1)n1nc(-c2ccc(Oc3ccccc3)cc2F)c2c(N)ncnc12)N1CCN(CC1)C1COC1 LCFFREMLXLZNHE-RUZDIDTESA-N 0.000 claims 1
- LCFFREMLXLZNHE-VWLOTQADSA-N 2-[(3s)-3-[4-amino-3-(2-fluoro-4-phenoxyphenyl)pyrazolo[3,4-d]pyrimidin-1-yl]piperidine-1-carbonyl]-4-methyl-4-[4-(oxetan-3-yl)piperazin-1-yl]pent-2-enenitrile Chemical compound C12=C(N)N=CN=C2N([C@H]2CCCN(C2)C(=O)C(C#N)=CC(C)(C)N2CCN(CC2)C2COC2)N=C1C(C(=C1)F)=CC=C1OC1=CC=CC=C1 LCFFREMLXLZNHE-VWLOTQADSA-N 0.000 claims 1
- MUZDXNQOSGWMJJ-UHFFFAOYSA-N 2-methylprop-2-enoic acid;prop-2-enoic acid Chemical compound OC(=O)C=C.CC(=C)C(O)=O MUZDXNQOSGWMJJ-UHFFFAOYSA-N 0.000 claims 1
- LQJBNNIYVWPHFW-UHFFFAOYSA-N 20:1omega9c fatty acid Natural products CCCCCCCCCCC=CCCCCCCCC(O)=O LQJBNNIYVWPHFW-UHFFFAOYSA-N 0.000 claims 1
- RWHRFHQRVDUPIK-UHFFFAOYSA-N 50867-57-7 Chemical compound CC(=C)C(O)=O.CC(=C)C(O)=O RWHRFHQRVDUPIK-UHFFFAOYSA-N 0.000 claims 1
- QSBYPNXLFMSGKH-UHFFFAOYSA-N 9-Heptadecensaeure Natural products CCCCCCCC=CCCCCCCCC(O)=O QSBYPNXLFMSGKH-UHFFFAOYSA-N 0.000 claims 1
- 208000032194 Acute haemorrhagic leukoencephalitis Diseases 0.000 claims 1
- 208000008822 Ankylosis Diseases 0.000 claims 1
- 208000032116 Autoimmune Experimental Encephalomyelitis Diseases 0.000 claims 1
- 208000023275 Autoimmune disease Diseases 0.000 claims 1
- 206010061666 Autonomic neuropathy Diseases 0.000 claims 1
- 208000003950 B-cell lymphoma Diseases 0.000 claims 1
- 208000028564 B-cell non-Hodgkin lymphoma Diseases 0.000 claims 1
- 208000032568 B-cell prolymphocytic leukaemia Diseases 0.000 claims 1
- 208000023611 Burkitt leukaemia Diseases 0.000 claims 1
- MWAPCVRIQHXPBI-UHFFFAOYSA-N CC(C=CC#N)(C)N1CCN(CC1)C1COC1 Chemical compound CC(C=CC#N)(C)N1CCN(CC1)C1COC1 MWAPCVRIQHXPBI-UHFFFAOYSA-N 0.000 claims 1
- 229920000623 Cellulose acetate phthalate Polymers 0.000 claims 1
- 229920003135 Eudragit® L 100-55 Polymers 0.000 claims 1
- 229920003138 Eudragit® L 30 D-55 Polymers 0.000 claims 1
- 208000035895 Guillain-Barré syndrome Diseases 0.000 claims 1
- 208000035186 Hemolytic Autoimmune Anemia Diseases 0.000 claims 1
- 206010023198 Joint ankylosis Diseases 0.000 claims 1
- 201000010743 Lambert-Eaton myasthenic syndrome Diseases 0.000 claims 1
- 208000031671 Large B-Cell Diffuse Lymphoma Diseases 0.000 claims 1
- 206010052178 Lymphocytic lymphoma Diseases 0.000 claims 1
- 201000003791 MALT lymphoma Diseases 0.000 claims 1
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- 206010029461 Nodal marginal zone B-cell lymphomas Diseases 0.000 claims 1
- ZQPPMHVWECSIRJ-UHFFFAOYSA-N Oleic acid Natural products CCCCCCCCC=CCCCCCCCC(O)=O ZQPPMHVWECSIRJ-UHFFFAOYSA-N 0.000 claims 1
- 239000005642 Oleic acid Substances 0.000 claims 1
- 208000005225 Opsoclonus-Myoclonus Syndrome Diseases 0.000 claims 1
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- 241000721454 Pemphigus Species 0.000 claims 1
- 208000007452 Plasmacytoma Diseases 0.000 claims 1
- 208000035416 Prolymphocytic B-Cell Leukemia Diseases 0.000 claims 1
- 201000004681 Psoriasis Diseases 0.000 claims 1
- 201000001263 Psoriatic Arthritis Diseases 0.000 claims 1
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- 208000005793 Restless legs syndrome Diseases 0.000 claims 1
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- 208000033559 Waldenström macroglobulinemia Diseases 0.000 claims 1
- ZUAAPNNKRHMPKG-UHFFFAOYSA-N acetic acid;butanedioic acid;methanol;propane-1,2-diol Chemical compound OC.CC(O)=O.CC(O)CO.OC(=O)CCC(O)=O ZUAAPNNKRHMPKG-UHFFFAOYSA-N 0.000 claims 1
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- QXJSBBXBKPUZAA-UHFFFAOYSA-N isooleic acid Natural products CCCCCCCC=CCCCCCCCCC(O)=O QXJSBBXBKPUZAA-UHFFFAOYSA-N 0.000 claims 1
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- ZQPPMHVWECSIRJ-KTKRTIGZSA-N oleic acid Chemical compound CCCCCCCC\C=C/CCCCCCCC(O)=O ZQPPMHVWECSIRJ-KTKRTIGZSA-N 0.000 claims 1
- 239000000546 pharmaceutical excipient Substances 0.000 claims 1
- 229920000642 polymer Polymers 0.000 claims 1
- 229920000136 polysorbate Polymers 0.000 claims 1
- 229920000036 polyvinylpyrrolidone Polymers 0.000 claims 1
- 239000001267 polyvinylpyrrolidone Substances 0.000 claims 1
- 235000013855 polyvinylpyrrolidone Nutrition 0.000 claims 1
- 206010039073 rheumatoid arthritis Diseases 0.000 claims 1
- JNYAEWCLZODPBN-CTQIIAAMSA-N sorbitan Polymers OCC(O)C1OCC(O)[C@@H]1O JNYAEWCLZODPBN-CTQIIAAMSA-N 0.000 claims 1
- 206010062113 splenic marginal zone lymphoma Diseases 0.000 claims 1
- KDYFGRWQOYBRFD-UHFFFAOYSA-L succinate(2-) Chemical compound [O-]C(=O)CCC([O-])=O KDYFGRWQOYBRFD-UHFFFAOYSA-L 0.000 claims 1
- 208000011580 syndromic disease Diseases 0.000 claims 1
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- 208000009174 transverse myelitis Diseases 0.000 claims 1
- 125000005591 trimellitate group Chemical group 0.000 claims 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201662356345P | 2016-06-29 | 2016-06-29 | |
| US62/356,345 | 2016-06-29 | ||
| PCT/US2017/040075 WO2018005849A1 (en) | 2016-06-29 | 2017-06-29 | Modified release formulations of 2-[3-[4-amino-3-(2-fluoro-4-phenoxy-phenyl)pyrazolo[3,4-d]pyrimidin-1-yl]piperidine-1-carbonyl]-4-methyl-4-[4-(oxetan-3-yl)piperazin-1-yl]pent-2-enenitrile |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2019519581A JP2019519581A (ja) | 2019-07-11 |
| JP2019519581A5 true JP2019519581A5 (enExample) | 2020-08-13 |
| JP7129704B2 JP7129704B2 (ja) | 2022-09-02 |
Family
ID=59315766
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2018568426A Active JP7129704B2 (ja) | 2016-06-29 | 2017-06-29 | ２－［３－［４－アミノ－３－（２－フルオロ－４－フェノキシ－フェニル）ピラゾロ［３，４－ｄ］ピリミジン－１－イル］ピペリジン－１－カルボニル］－４－メチル－４－［４－（オキセタン－３－イル）ピペラジン－１－イル］ペント－２－エネニトリルの放出調節製剤 |
Country Status (14)
| Country | Link |
|---|---|
| US (3) | US20190231784A1 (enExample) |
| EP (1) | EP3478273A1 (enExample) |
| JP (1) | JP7129704B2 (enExample) |
| KR (2) | KR102391693B1 (enExample) |
| CN (2) | CN109600989B (enExample) |
| AU (2) | AU2017290354C1 (enExample) |
| CA (1) | CA3028169C (enExample) |
| EA (1) | EA201892836A1 (enExample) |
| IL (2) | IL293621B2 (enExample) |
| MA (1) | MA45547A (enExample) |
| MX (2) | MX390619B (enExample) |
| NZ (1) | NZ749662A (enExample) |
| SG (1) | SG11201811255WA (enExample) |
| WO (1) | WO2018005849A1 (enExample) |
Families Citing this family (25)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| SG11201501815UA (en) | 2012-09-10 | 2015-05-28 | Principia Biopharma Inc | Pyrazolopyrimidine compounds as kinase inhibitors |
| KR20160117614A (ko) | 2014-02-21 | 2016-10-10 | 프린시피아 바이오파마, 인코퍼레이티드 | Btk 억제제의 염 및 고체 형태 |
| AU2015364335B2 (en) | 2014-12-18 | 2020-11-26 | Principia Biopharma Inc. | Treatment of pemphigus |
| EP3313839A1 (en) | 2015-06-24 | 2018-05-02 | Principia Biopharma Inc. | Tyrosine kinase inhibitors |
| IL293621B2 (en) | 2016-06-29 | 2023-09-01 | Principia Biopharma Inc | Modified release formulations of 2-[3-[4-amino-3-(2-fluoro-4-phenoxy-phenyl)pyrazolo[4,3-d]pyrimidin-1-yl]piperidine-1-carbonyl]-4 -Methyl-4-[4-(oxane-3-yl)piperazine-1-yl)penta-2-ananitrile |
| JP7555327B2 (ja) | 2018-07-25 | 2024-09-24 | ノバルティス アーゲー | Ｎｌｒｐ３インフラマソーム阻害剤 |
| MY208604A (en) | 2018-12-14 | 2025-05-20 | Chia Tai Tianqing Pharmaceutical Group Co Ltd | Salt of syk inhibitor and crystalline form thereof |
| AR119731A1 (es) | 2019-05-17 | 2022-01-05 | Novartis Ag | Inhibidores del inflamasoma nlrp3 |
| CA3153750A1 (en) | 2019-10-09 | 2021-04-15 | Ann NEALE | Methods of treating pemphigus by administering (r)-2-[3-[4-amino-3-(2-fluoro-4-phenoxy-phenyl)pyrazolo[3,4-d]pyrimidin-1-yl]piperidine-1-carbonyl]-4-methyl-4-[4-(oxetan-3-yl)piperazin-1-yl]pent-2-enenitrile |
| CN115209899A (zh) | 2019-10-14 | 2022-10-18 | 普林斯匹亚生物制药公司 | 通过施用(R)-2-[3-[4-氨基-3-(2-氟-4-苯氧基-苯基)吡唑并[3,4-d]嘧啶-1-基]哌啶-1-羰基]-4-甲基-4-[4-(氧杂环丁-3-基)哌嗪-1-基]戊-2-烯腈治疗免疫性血小板减少症的方法 |
| BR112022011950A2 (pt) * | 2020-01-06 | 2022-09-06 | Principia Biopharma Inc | Tratamento da nefropatia membranosa, doença relacionada ao igg4, e síndrome antifosfolipídica usando o inibidor btk 2-[(3r)-3-[4-4-amino-3-(2-fluoro-4-4-fenoxi-fenil)pirazolo[3], 4-4-d]pyrimidin-1-yl]piperidina-1-carbonil]-4-4-metil-4-4-[4-4-(oxetan-3-yl)piperazin-1-il]pent-2-enenitrila |
| AU2021205248A1 (en) * | 2020-01-08 | 2022-09-01 | Principia Biopharma Inc. | Topical pharmaceutical compositions comprising 2-[3-[4-amino-3-(2-fluoro-4-phenoxy-phenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl]piperidine-1-carbonyl]-4,4-dimethylpent-2-enenitrile |
| EP4093741A1 (en) | 2020-01-22 | 2022-11-30 | Principia Biopharma Inc. | Crystalline forms of 2-[3-[4-amino-3-(2-fluoro-4-phenoxy-phenyl)-1h-pyrazolo[3,4-d]pyrimidin-1-yl]piperidine-1-carbonyl]-4-methyl-4-[4-(oxetan-3-yl)piperazin-1-yl]pent-2-enenitrile |
| TW202214250A (zh) * | 2020-08-10 | 2022-04-16 | 大陸商江蘇恆瑞醫藥股份有限公司 | Ｂｔｋ抑制劑治療疾病的用途 |
| WO2022034529A1 (en) | 2020-08-14 | 2022-02-17 | Novartis Ag | Heteroaryl substituted spiropiperidinyl derivatives and pharmaceutical uses thereof |
| BR112023018570A2 (pt) | 2021-04-16 | 2023-11-28 | Principia Biopharma Inc | Métodos para o tratamento de trombocitopenia imune induzida por fármacos e vacinas através da administração de compostos específicos |
| KR20240129063A (ko) * | 2022-01-13 | 2024-08-27 | 앰릿 엔도우, 인크. | 경구 투여 형태 |
| UY40374A (es) | 2022-08-03 | 2024-02-15 | Novartis Ag | Inhibidores de inflamasoma nlrp3 |
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| CN110483521B (zh) | 2018-05-14 | 2022-06-07 | 杭州和正医药有限公司 | 一种可逆共价布鲁顿酪氨酸激酶抑制剂、药物组合物及其应用 |
| CN115209899A (zh) | 2019-10-14 | 2022-10-18 | 普林斯匹亚生物制药公司 | 通过施用(R)-2-[3-[4-氨基-3-(2-氟-4-苯氧基-苯基)吡唑并[3,4-d]嘧啶-1-基]哌啶-1-羰基]-4-甲基-4-[4-(氧杂环丁-3-基)哌嗪-1-基]戊-2-烯腈治疗免疫性血小板减少症的方法 |
| EP4093741A1 (en) | 2020-01-22 | 2022-11-30 | Principia Biopharma Inc. | Crystalline forms of 2-[3-[4-amino-3-(2-fluoro-4-phenoxy-phenyl)-1h-pyrazolo[3,4-d]pyrimidin-1-yl]piperidine-1-carbonyl]-4-methyl-4-[4-(oxetan-3-yl)piperazin-1-yl]pent-2-enenitrile |
| WO2022081512A1 (en) | 2020-10-12 | 2022-04-21 | Synubi Pharmaceuticals Llc | Compositions and methods of treatment of neuroinflammatory diseases with bruton's tyrosine kinase inhibitors |
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2017
- 2017-06-29 IL IL293621A patent/IL293621B2/en unknown
- 2017-06-29 EP EP17738009.4A patent/EP3478273A1/en active Pending
- 2017-06-29 NZ NZ749662A patent/NZ749662A/en unknown
- 2017-06-29 EA EA201892836A patent/EA201892836A1/ru unknown
- 2017-06-29 KR KR1020197002895A patent/KR102391693B1/ko active Active
- 2017-06-29 SG SG11201811255WA patent/SG11201811255WA/en unknown
- 2017-06-29 AU AU2017290354A patent/AU2017290354C1/en active Active
- 2017-06-29 KR KR1020227013784A patent/KR102515813B1/ko active Active
- 2017-06-29 US US16/312,258 patent/US20190231784A1/en not_active Abandoned
- 2017-06-29 IL IL263815A patent/IL263815B/en unknown
- 2017-06-29 MA MA045547A patent/MA45547A/fr unknown
- 2017-06-29 MX MX2018016056A patent/MX390619B/es unknown
- 2017-06-29 CA CA3028169A patent/CA3028169C/en active Active
- 2017-06-29 JP JP2018568426A patent/JP7129704B2/ja active Active
- 2017-06-29 CN CN201780049475.1A patent/CN109600989B/zh active Active
- 2017-06-29 WO PCT/US2017/040075 patent/WO2018005849A1/en not_active Ceased
- 2017-06-29 CN CN202210686970.6A patent/CN115054586B/zh active Active
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2018
- 2018-12-18 MX MX2022002952A patent/MX2022002952A/es unknown
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2020
- 2020-10-28 US US17/082,747 patent/US11872229B2/en active Active
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2023
- 2023-03-17 AU AU2023201685A patent/AU2023201685A1/en not_active Abandoned
- 2023-12-01 US US18/526,225 patent/US12336999B2/en active Active
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