EA201892836A1 - Составы 2-[3-[4-амино-3-(2-фтор-4-феноксифенил)пиразол[3,4-d]пиримидин-1-ил]пиперидин-1-карбонил]-4-метил-4-[4-(оксетан-3-ил)пиперазин-1-ил]пент-2-еннитрила с модифицированным высвобождением - Google Patents
Составы 2-[3-[4-амино-3-(2-фтор-4-феноксифенил)пиразол[3,4-d]пиримидин-1-ил]пиперидин-1-карбонил]-4-метил-4-[4-(оксетан-3-ил)пиперазин-1-ил]пент-2-еннитрила с модифицированным высвобождениемInfo
- Publication number
- EA201892836A1 EA201892836A1 EA201892836A EA201892836A EA201892836A1 EA 201892836 A1 EA201892836 A1 EA 201892836A1 EA 201892836 A EA201892836 A EA 201892836A EA 201892836 A EA201892836 A EA 201892836A EA 201892836 A1 EA201892836 A1 EA 201892836A1
- Authority
- EA
- Eurasian Patent Office
- Prior art keywords
- modified release
- ennitril
- oxetan
- phenoxyphenyl
- pent
- Prior art date
Links
- 239000000203 mixture Substances 0.000 title abstract 6
- -1 2-fluoro-4-phenoxyphenyl Chemical group 0.000 title 1
- WTKZEGDFNFYCGP-UHFFFAOYSA-N Pyrazole Chemical compound C=1C=NNC=1 WTKZEGDFNFYCGP-UHFFFAOYSA-N 0.000 title 1
- ISBHMJZRKAFTGE-UHFFFAOYSA-N pent-2-enenitrile Chemical compound CCC=CC#N ISBHMJZRKAFTGE-UHFFFAOYSA-N 0.000 title 1
- 239000011248 coating agent Substances 0.000 abstract 3
- 238000000576 coating method Methods 0.000 abstract 3
- OUYCCCASQSFEME-QMMMGPOBSA-N L-tyrosine Chemical compound OC(=O)[C@@H](N)CC1=CC=C(O)C=C1 OUYCCCASQSFEME-QMMMGPOBSA-N 0.000 abstract 2
- 239000002702 enteric coating Substances 0.000 abstract 2
- 238000009505 enteric coating Methods 0.000 abstract 2
- 238000009472 formulation Methods 0.000 abstract 2
- 239000010410 layer Substances 0.000 abstract 2
- OUYCCCASQSFEME-UHFFFAOYSA-N tyrosine Natural products OC(=O)C(N)CC1=CC=C(O)C=C1 OUYCCCASQSFEME-UHFFFAOYSA-N 0.000 abstract 2
- WROUWQQRXUBECT-UHFFFAOYSA-N 2-ethylacrylic acid Chemical compound CCC(=C)C(O)=O WROUWQQRXUBECT-UHFFFAOYSA-N 0.000 abstract 1
- CERQOIWHTDAKMF-UHFFFAOYSA-N Methacrylic acid Chemical compound CC(=C)C(O)=O CERQOIWHTDAKMF-UHFFFAOYSA-N 0.000 abstract 1
- 239000004372 Polyvinyl alcohol Substances 0.000 abstract 1
- NIXOWILDQLNWCW-UHFFFAOYSA-N acrylic acid group Chemical group C(C=C)(=O)O NIXOWILDQLNWCW-UHFFFAOYSA-N 0.000 abstract 1
- 239000001913 cellulose Substances 0.000 abstract 1
- 229920002678 cellulose Polymers 0.000 abstract 1
- 150000001875 compounds Chemical class 0.000 abstract 1
- 229920001577 copolymer Polymers 0.000 abstract 1
- 229920001519 homopolymer Polymers 0.000 abstract 1
- 239000001866 hydroxypropyl methyl cellulose Substances 0.000 abstract 1
- 229920003088 hydroxypropyl methyl cellulose Polymers 0.000 abstract 1
- 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 abstract 1
- 235000010979 hydroxypropyl methyl cellulose Nutrition 0.000 abstract 1
- 239000003112 inhibitor Substances 0.000 abstract 1
- 238000000034 method Methods 0.000 abstract 1
- 229920000642 polymer Polymers 0.000 abstract 1
- 229920002451 polyvinyl alcohol Polymers 0.000 abstract 1
- 229920000036 polyvinylpyrrolidone Polymers 0.000 abstract 1
- 239000001267 polyvinylpyrrolidone Substances 0.000 abstract 1
- 235000013855 polyvinylpyrrolidone Nutrition 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 239000007909 solid dosage form Substances 0.000 abstract 1
Classifications
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- A—HUMAN NECESSITIES
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- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
-
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- A61K9/2004—Excipients; Inactive ingredients
- A61K9/2013—Organic compounds, e.g. phospholipids, fats
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Abstract
Составы с модифицированным высвобождением, такие как твердые лекарственные формы для перорального применения, содержащие композицию сердцевины, содержащую соединение (I) и/или его фармацевтически приемлемую соль; подслой покрытия, покрывающий композицию сердцевины, причем указанный подслой покрытия содержит поливиниловый спирт и/или гидроксипропилметилцеллюлозу; и слой кишечнорастворимого покрытия, инкапсулирующий подслой покрытия и композицию сердцевины, причем указанный слой кишечнорастворимого покрытия содержит по меньшей мере один полимер, выбранный из гомополимера акриловой/метакриловой/этакриловой кислоты и их сополимеров, производного целлюлозы и поливинилпирролидона, и способы введения ингибитора тирозинкиназы Брутона (ВТК) с использованием указанных составов.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201662356345P | 2016-06-29 | 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 (1)
| Publication Number | Publication Date |
|---|---|
| EA201892836A1 true EA201892836A1 (ru) | 2019-07-31 |
Family
ID=59315766
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| EA201892836A EA201892836A1 (ru) | 2016-06-29 | 2017-06-29 | Составы 2-[3-[4-амино-3-(2-фтор-4-феноксифенил)пиразол[3,4-d]пиримидин-1-ил]пиперидин-1-карбонил]-4-метил-4-[4-(оксетан-3-ил)пиперазин-1-ил]пент-2-еннитрила с модифицированным высвобождением |
Country Status (13)
| Country | Link |
|---|---|
| US (4) | US20190231784A1 (ru) |
| EP (1) | EP3478273A1 (ru) |
| JP (1) | JP7129704B2 (ru) |
| KR (2) | KR102391693B1 (ru) |
| CN (2) | CN109600989B (ru) |
| AU (2) | AU2017290354C1 (ru) |
| CA (1) | CA3028169C (ru) |
| EA (1) | EA201892836A1 (ru) |
| IL (2) | IL293621B2 (ru) |
| MA (1) | MA45547A (ru) |
| MX (2) | MX390619B (ru) |
| SG (1) | SG11201811255WA (ru) |
| WO (1) | WO2018005849A1 (ru) |
Families Citing this family (27)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| RS58956B1 (sr) | 2012-09-10 | 2019-08-30 | Principia Biopharma Inc | Jedinjenja pirazolopirimidina kao inhibitori kinaze |
| MX372673B (es) | 2014-02-21 | 2020-03-25 | Principia Biopharma Inc | Un inhibidor de btk para usarse en el tratamiento de penfigo y sales y formas sólidas del mismo. |
| ES2843323T3 (es) | 2014-12-18 | 2021-07-16 | Principia Biopharma Inc | Tratamiento de pénfigo |
| EP3313839A1 (en) | 2015-06-24 | 2018-05-02 | Principia Biopharma Inc. | Tyrosine kinase inhibitors |
| US20190231784A1 (en) | 2016-06-29 | 2019-08-01 | Principia Biopharma Inc. | 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 |
| JOP20210017A1 (ar) | 2018-07-25 | 2021-01-21 | Novartis Ag | مثبطات جسيم التهابي nlrp3 |
| SG11202106210QA (en) | 2018-12-14 | 2021-07-29 | Chia Tai Tianqing Pharmaceutical Group Co Ltd | Salt of syk inhibitor and crystalline form thereof |
| UY38687A (es) | 2019-05-17 | 2023-05-15 | Novartis Ag | Inhibidores del inflamasoma nlrp3, composiciones, combinaciones de los mismos y métodos para su uso |
| 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 |
| KR20220080179A (ko) | 2019-10-14 | 2022-06-14 | 프린시피아 바이오파마, 인코퍼레이티드 | (R)-2-[3-[4-아미노-3-(2-플루오로-4-페녹시-페닐)피라졸로[3,4-d]피리미딘-1-일]피페리딘-1-카르보닐]-4-메틸-4-[4-(옥세탄-3-일)피페라진-1-일]펜트-2-엔니트릴을 투여하여 면역 혈소판 감소증을 치료하는 방법 |
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| TWI810582B (zh) | 2015-06-03 | 2023-08-01 | 美商普林斯匹亞生物製藥公司 | 酪胺酸激酶抑制劑 |
| EP3313839A1 (en) | 2015-06-24 | 2018-05-02 | Principia Biopharma Inc. | Tyrosine kinase inhibitors |
| CN105753863B (zh) | 2015-09-11 | 2018-07-31 | 东莞市真兴贝特医药技术有限公司 | 氧代二氢咪唑并吡啶类化合物及其应用 |
| US10358446B2 (en) | 2015-10-14 | 2019-07-23 | Zibo Biopolar Changsheng Pharmaceutical Co., Ltd. | Bruton's tyrosine kinase inhibitors |
| US20190231784A1 (en) | 2016-06-29 | 2019-08-01 | Principia Biopharma Inc. | 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 |
| EP3789040A4 (en) | 2018-04-27 | 2022-03-09 | ONO Pharmaceutical Co., Ltd. | PREVENTIVE AND/OR THERAPEUTIC AGENT FOR AUTOIMMUNE DISEASES WITH A COMPOUND WITH BTK INHIBITING ACTIVITY AS AN INGREDIENT |
| 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 |
| KR20220080179A (ko) | 2019-10-14 | 2022-06-14 | 프린시피아 바이오파마, 인코퍼레이티드 | (R)-2-[3-[4-아미노-3-(2-플루오로-4-페녹시-페닐)피라졸로[3,4-d]피리미딘-1-일]피페리딘-1-카르보닐]-4-메틸-4-[4-(옥세탄-3-일)피페라진-1-일]펜트-2-엔니트릴을 투여하여 면역 혈소판 감소증을 치료하는 방법 |
| TW202140484A (zh) | 2020-01-22 | 2021-11-01 | 美商普林斯匹亞生物製藥公司 | 2-[3-[4-胺基-3-(2-氟-4-苯氧基-苯基)-1H-吡唑并[3,4-d]嘧啶-1-基]哌啶-1-羰基]-4-甲基-4-[4-(氧環丁烷-3-基)哌𠯤-1-基]戊-2-烯腈之晶形 |
| 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 |
-
2017
- 2017-06-29 US US16/312,258 patent/US20190231784A1/en not_active Abandoned
- 2017-06-29 IL IL293621A patent/IL293621B2/en unknown
- 2017-06-29 KR KR1020197002895A patent/KR102391693B1/ko active Active
- 2017-06-29 IL IL263815A patent/IL263815B/en unknown
- 2017-06-29 MA MA045547A patent/MA45547A/fr unknown
- 2017-06-29 EP EP17738009.4A patent/EP3478273A1/en active Pending
- 2017-06-29 EA EA201892836A patent/EA201892836A1/ru unknown
- 2017-06-29 WO PCT/US2017/040075 patent/WO2018005849A1/en not_active Ceased
- 2017-06-29 KR KR1020227013784A patent/KR102515813B1/ko active Active
- 2017-06-29 MX MX2018016056A patent/MX390619B/es unknown
- 2017-06-29 AU AU2017290354A patent/AU2017290354C1/en active Active
- 2017-06-29 CN CN201780049475.1A patent/CN109600989B/zh active Active
- 2017-06-29 JP JP2018568426A patent/JP7129704B2/ja active Active
- 2017-06-29 CA CA3028169A patent/CA3028169C/en active Active
- 2017-06-29 SG SG11201811255WA patent/SG11201811255WA/en unknown
- 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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2025
- 2025-05-23 US US19/217,161 patent/US20250381193A1/en active Pending
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