JP2018500353A5 - - Google Patents
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- Publication number
- JP2018500353A5 JP2018500353A5 JP2017533932A JP2017533932A JP2018500353A5 JP 2018500353 A5 JP2018500353 A5 JP 2018500353A5 JP 2017533932 A JP2017533932 A JP 2017533932A JP 2017533932 A JP2017533932 A JP 2017533932A JP 2018500353 A5 JP2018500353 A5 JP 2018500353A5
- Authority
- JP
- Japan
- Prior art keywords
- solid oral
- pharmaceutically acceptable
- water
- compound
- oral preparation
- 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
- 239000007787 solid Substances 0.000 claims 30
- 238000002360 preparation method Methods 0.000 claims 18
- 150000001875 compounds Chemical class 0.000 claims 16
- 239000000203 mixture Substances 0.000 claims 15
- 150000003839 salts Chemical class 0.000 claims 12
- 238000009472 formulation Methods 0.000 claims 10
- 239000002245 particle Substances 0.000 claims 7
- 229920002678 cellulose Polymers 0.000 claims 6
- 239000001913 cellulose Substances 0.000 claims 6
- 235000010980 cellulose Nutrition 0.000 claims 6
- 239000002702 enteric coating Substances 0.000 claims 6
- 238000009505 enteric coating Methods 0.000 claims 6
- 239000007864 aqueous solution Substances 0.000 claims 5
- 229920003063 hydroxymethyl cellulose Polymers 0.000 claims 4
- 229940031574 hydroxymethyl cellulose Drugs 0.000 claims 4
- 229920003088 hydroxypropyl methyl cellulose Polymers 0.000 claims 4
- 235000010979 hydroxypropyl methyl cellulose Nutrition 0.000 claims 4
- 229920000642 polymer Polymers 0.000 claims 4
- KDYFGRWQOYBRFD-UHFFFAOYSA-L succinate(2-) Chemical compound [O-]C(=O)CCC([O-])=O KDYFGRWQOYBRFD-UHFFFAOYSA-L 0.000 claims 4
- QTBSBXVTEAMEQO-UHFFFAOYSA-N Acetic acid Chemical compound CC(O)=O QTBSBXVTEAMEQO-UHFFFAOYSA-N 0.000 claims 3
- 229920000623 Cellulose acetate phthalate Polymers 0.000 claims 3
- VVQNEPGJFQJSBK-UHFFFAOYSA-N Methyl methacrylate Chemical compound COC(=O)C(C)=C VVQNEPGJFQJSBK-UHFFFAOYSA-N 0.000 claims 3
- 239000012736 aqueous medium Substances 0.000 claims 3
- 229940081734 cellulose acetate phthalate Drugs 0.000 claims 3
- 238000004090 dissolution Methods 0.000 claims 3
- 239000001866 hydroxypropyl methyl cellulose Substances 0.000 claims 3
- 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 3
- 239000000178 monomer Substances 0.000 claims 3
- XNGIFLGASWRNHJ-UHFFFAOYSA-L phthalate(2-) Chemical compound [O-]C(=O)C1=CC=CC=C1C([O-])=O XNGIFLGASWRNHJ-UHFFFAOYSA-L 0.000 claims 3
- 229920001451 polypropylene glycol Polymers 0.000 claims 3
- 229940100467 polyvinyl acetate phthalate Drugs 0.000 claims 3
- 229920003134 Eudragit® polymer Polymers 0.000 claims 2
- 241000124008 Mammalia Species 0.000 claims 2
- BAPJBEWLBFYGME-UHFFFAOYSA-N Methyl acrylate Chemical group COC(=O)C=C BAPJBEWLBFYGME-UHFFFAOYSA-N 0.000 claims 2
- 239000002202 Polyethylene glycol Substances 0.000 claims 2
- 229920001577 copolymer Polymers 0.000 claims 2
- 201000010099 disease Diseases 0.000 claims 2
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 2
- 150000004676 glycans Chemical class 0.000 claims 2
- 229920003132 hydroxypropyl methylcellulose phthalate Polymers 0.000 claims 2
- 239000006186 oral dosage form Substances 0.000 claims 2
- 239000000546 pharmaceutical excipient Substances 0.000 claims 2
- 229920001223 polyethylene glycol Polymers 0.000 claims 2
- 229920001282 polysaccharide Polymers 0.000 claims 2
- 239000005017 polysaccharide Substances 0.000 claims 2
- 229920002744 polyvinyl acetate phthalate Polymers 0.000 claims 2
- 239000004094 surface-active agent Substances 0.000 claims 2
- ARCGXLSVLAOJQL-UHFFFAOYSA-N trimellitic acid Chemical compound OC(=O)C1=CC=C(C(O)=O)C(C(O)=O)=C1 ARCGXLSVLAOJQL-UHFFFAOYSA-N 0.000 claims 2
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 claims 2
- QTBSBXVTEAMEQO-UHFFFAOYSA-M Acetate Chemical compound CC([O-])=O QTBSBXVTEAMEQO-UHFFFAOYSA-M 0.000 claims 1
- 208000023275 Autoimmune disease Diseases 0.000 claims 1
- JIGUQPWFLRLWPJ-UHFFFAOYSA-N Ethyl acrylate Chemical compound CCOC(=O)C=C JIGUQPWFLRLWPJ-UHFFFAOYSA-N 0.000 claims 1
- 108010010803 Gelatin Proteins 0.000 claims 1
- 229920000663 Hydroxyethyl cellulose Polymers 0.000 claims 1
- 239000004354 Hydroxyethyl cellulose Substances 0.000 claims 1
- 229920002153 Hydroxypropyl cellulose Polymers 0.000 claims 1
- CERQOIWHTDAKMF-UHFFFAOYSA-N Methacrylic acid Chemical compound CC(=C)C(O)=O CERQOIWHTDAKMF-UHFFFAOYSA-N 0.000 claims 1
- 229920000168 Microcrystalline cellulose Polymers 0.000 claims 1
- 206010028980 Neoplasm Diseases 0.000 claims 1
- 229920002845 Poly(methacrylic acid) Polymers 0.000 claims 1
- 239000004372 Polyvinyl alcohol Substances 0.000 claims 1
- 229920001800 Shellac Polymers 0.000 claims 1
- 229920002125 Sokalan® Polymers 0.000 claims 1
- 239000002253 acid Substances 0.000 claims 1
- 230000002378 acidificating effect Effects 0.000 claims 1
- 239000000853 adhesive Substances 0.000 claims 1
- 239000003463 adsorbent Substances 0.000 claims 1
- 230000000181 anti-adherent effect Effects 0.000 claims 1
- 239000002518 antifoaming agent Substances 0.000 claims 1
- 239000003963 antioxidant agent Substances 0.000 claims 1
- 230000003078 antioxidant effect Effects 0.000 claims 1
- 239000011230 binding agent Substances 0.000 claims 1
- 229920001400 block copolymer Polymers 0.000 claims 1
- 201000011510 cancer Diseases 0.000 claims 1
- 239000002775 capsule Substances 0.000 claims 1
- 230000015556 catabolic process Effects 0.000 claims 1
- 239000003795 chemical substances by application Substances 0.000 claims 1
- 239000003086 colorant Substances 0.000 claims 1
- 238000006731 degradation reaction Methods 0.000 claims 1
- 238000009792 diffusion process Methods 0.000 claims 1
- 239000003085 diluting agent Substances 0.000 claims 1
- 239000007884 disintegrant Substances 0.000 claims 1
- SUPCQIBBMFXVTL-UHFFFAOYSA-N ethyl 2-methylprop-2-enoate Chemical compound CCOC(=O)C(C)=C SUPCQIBBMFXVTL-UHFFFAOYSA-N 0.000 claims 1
- 239000000945 filler Substances 0.000 claims 1
- 239000000796 flavoring agent Substances 0.000 claims 1
- 239000012530 fluid Substances 0.000 claims 1
- 235000013355 food flavoring agent Nutrition 0.000 claims 1
- 235000003599 food sweetener Nutrition 0.000 claims 1
- 210000001035 gastrointestinal tract Anatomy 0.000 claims 1
- 229920000159 gelatin Polymers 0.000 claims 1
- 239000008273 gelatin Substances 0.000 claims 1
- 229940014259 gelatin Drugs 0.000 claims 1
- 235000019322 gelatine Nutrition 0.000 claims 1
- 235000011852 gelatine desserts Nutrition 0.000 claims 1
- 235000019447 hydroxyethyl cellulose Nutrition 0.000 claims 1
- 229940071826 hydroxyethyl cellulose Drugs 0.000 claims 1
- 239000001863 hydroxypropyl cellulose Substances 0.000 claims 1
- 235000010977 hydroxypropyl cellulose Nutrition 0.000 claims 1
- 229940031704 hydroxypropyl methylcellulose phthalate Drugs 0.000 claims 1
- 229940071676 hydroxypropylcellulose Drugs 0.000 claims 1
- 208000027866 inflammatory disease Diseases 0.000 claims 1
- 230000005764 inhibitory process Effects 0.000 claims 1
- 230000000968 intestinal effect Effects 0.000 claims 1
- 239000000314 lubricant Substances 0.000 claims 1
- 229940117841 methacrylic acid copolymer Drugs 0.000 claims 1
- 229920003145 methacrylic acid copolymer Polymers 0.000 claims 1
- 229920000609 methyl cellulose Polymers 0.000 claims 1
- 239000001923 methylcellulose Substances 0.000 claims 1
- 229960002900 methylcellulose Drugs 0.000 claims 1
- 239000000693 micelle Substances 0.000 claims 1
- 239000008108 microcrystalline cellulose Substances 0.000 claims 1
- 229940016286 microcrystalline cellulose Drugs 0.000 claims 1
- 235000019813 microcrystalline cellulose Nutrition 0.000 claims 1
- PNJWIWWMYCMZRO-UHFFFAOYSA-N pent‐4‐en‐2‐one Natural products CC(=O)CC=C PNJWIWWMYCMZRO-UHFFFAOYSA-N 0.000 claims 1
- XNGIFLGASWRNHJ-UHFFFAOYSA-M phthalate(1-) Chemical compound OC(=O)C1=CC=CC=C1C([O-])=O XNGIFLGASWRNHJ-UHFFFAOYSA-M 0.000 claims 1
- KQOCPYKMLMTOOP-UHFFFAOYSA-N phthalic acid;propanoic acid Chemical compound CCC(O)=O.OC(=O)C1=CC=CC=C1C(O)=O KQOCPYKMLMTOOP-UHFFFAOYSA-N 0.000 claims 1
- 239000004014 plasticizer Substances 0.000 claims 1
- 229920002451 polyvinyl alcohol 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
- 239000003755 preservative agent Substances 0.000 claims 1
- 230000002335 preservative effect Effects 0.000 claims 1
- ZLGIYFNHBLSMPS-ATJNOEHPSA-N shellac Chemical compound OCCCCCC(O)C(O)CCCCCCCC(O)=O.C1C23[C@H](C(O)=O)CCC2[C@](C)(CO)[C@@H]1C(C(O)=O)=C[C@@H]3O ZLGIYFNHBLSMPS-ATJNOEHPSA-N 0.000 claims 1
- 229940113147 shellac Drugs 0.000 claims 1
- 239000004208 shellac Substances 0.000 claims 1
- 235000013874 shellac Nutrition 0.000 claims 1
- 210000000813 small intestine Anatomy 0.000 claims 1
- 239000003765 sweetening agent Substances 0.000 claims 1
- 230000008961 swelling Effects 0.000 claims 1
- 229920002554 vinyl polymer Polymers 0.000 claims 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201462096812P | 2014-12-24 | 2014-12-24 | |
| US62/096,812 | 2014-12-24 | ||
| PCT/US2015/000515 WO2016105582A1 (en) | 2014-12-24 | 2015-12-23 | Compositions for ileo-jejunal drug delivery |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2018500353A JP2018500353A (ja) | 2018-01-11 |
| JP2018500353A5 true JP2018500353A5 (enExample) | 2019-02-07 |
| JP6687248B2 JP6687248B2 (ja) | 2020-04-22 |
Family
ID=55361929
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2017533932A Active JP6687248B2 (ja) | 2014-12-24 | 2015-12-23 | 回腸−空腸薬物送達用組成物 |
Country Status (15)
| Country | Link |
|---|---|
| US (1) | US20180193274A1 (enExample) |
| EP (1) | EP3236943B1 (enExample) |
| JP (1) | JP6687248B2 (enExample) |
| DK (1) | DK3236943T3 (enExample) |
| ES (1) | ES2942642T3 (enExample) |
| FI (1) | FI3236943T3 (enExample) |
| HR (1) | HRP20230305T1 (enExample) |
| HU (1) | HUE061809T2 (enExample) |
| LT (1) | LT3236943T (enExample) |
| MA (1) | MA41265B1 (enExample) |
| PL (1) | PL3236943T3 (enExample) |
| PT (1) | PT3236943T (enExample) |
| RS (1) | RS64139B1 (enExample) |
| SI (1) | SI3236943T1 (enExample) |
| WO (1) | WO2016105582A1 (enExample) |
Families Citing this family (36)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| PL2892900T3 (pl) | 2012-09-10 | 2018-02-28 | Principia Biopharma Inc. | Związki pyrazolopirymidonowe jako inhibitory kinazy |
| SMT201700160T1 (it) | 2013-04-25 | 2017-05-08 | Beigene Ltd | Composti eterociclici fusi come inibitori di protein chinasi |
| ES2792183T3 (es) | 2013-09-13 | 2020-11-10 | Beigene Switzerland Gmbh | Anticuerpos anti-PD1 y su uso como productos terapéuticos y de diagnóstico |
| CA2939186C (en) | 2014-02-21 | 2023-03-07 | Principia Biopharma Inc. | Salts and solid form of a btk inhibitor |
| CN106604742B (zh) | 2014-07-03 | 2019-01-11 | 百济神州有限公司 | 抗pd-l1抗体及其作为治疗剂及诊断剂的用途 |
| US10485797B2 (en) | 2014-12-18 | 2019-11-26 | Principia Biopharma Inc. | Treatment of pemphigus |
| MA42242A (fr) | 2015-06-24 | 2018-05-02 | Principia Biopharma Inc | Inhibiteurs de la tyrosine kinase |
| SG11201809751XA (en) | 2016-05-26 | 2018-12-28 | Zeno Royalties & Milestones Llc | Egfr inhibitor compounds |
| MX390619B (es) | 2016-06-29 | 2025-03-21 | Principia Biopharma Inc | Formulaciones de liberacion modificada de 2-[3-[4-amino-3-(2-fluoro-4-fenoxi-fenil)pirazolo[3,4-d]pirimidin-1-il]piperidina-1-carbonil]-4-metil-4-[4-(oxetan-3-il)piperazin-1-il]pent-2-enenitrilo |
| CN109475536B (zh) | 2016-07-05 | 2022-05-27 | 百济神州有限公司 | 用于治疗癌症的PD-l拮抗剂和RAF抑制剂的组合 |
| WO2018033853A2 (en) | 2016-08-16 | 2018-02-22 | Beigene, Ltd. | Crystalline form of (s)-7-(1-acryloylpiperidin-4-yl)-2-(4-phenoxyphenyl)-4,5,6,7-tetra-hydropyrazolo[1,5-a]pyrimidine-3-carboxamide, preparation, and uses thereof |
| PT3500299T (pt) | 2016-08-19 | 2024-02-21 | Beigene Switzerland Gmbh | Combinação de zanubrutinib com um anticorpo anti-cd20 ou anti-pd-1 para utilização no tratamento do cancro |
| CN106588937B (zh) * | 2017-01-16 | 2018-09-21 | 东莞市真兴贝特医药技术有限公司 | 咪唑并吡嗪类化合物及其制备方法和应用 |
| CN110461847B (zh) | 2017-01-25 | 2022-06-07 | 百济神州有限公司 | (S)-7-(1-(丁-2-炔酰基)哌啶-4-基)-2-(4-苯氧基苯基)-4,5,6,7-四氢吡唑并[1,5-a]嘧啶-3-甲酰胺的结晶形式、其制备及用途 |
| TW202515616A (zh) | 2017-06-26 | 2025-04-16 | 英屬開曼群島商百濟神州有限公司 | 抗pd-1抗體或其抗原結合片段在製備治療用於患有肝細胞癌(hcc)之藥物的用途 |
| CN110997677A (zh) | 2017-08-12 | 2020-04-10 | 百济神州有限公司 | 具有改进的双重选择性的Btk抑制剂 |
| CN114478544B (zh) * | 2017-09-28 | 2023-06-16 | 上海海雁医药科技有限公司 | 4,6,7-三取代1,2-二氢吡咯并[3,4-c]吡啶/嘧啶-3-酮衍生物及用途 |
| WO2019108795A1 (en) | 2017-11-29 | 2019-06-06 | Beigene Switzerland Gmbh | Treatment of indolent or aggressive b-cell lymphomas using a combination comprising btk inhibitors |
| US11576917B2 (en) | 2018-01-20 | 2023-02-14 | Natco Pharma Limited | Pharmaceutical compositions comprising Ibrutinib |
| KR102328682B1 (ko) | 2018-08-27 | 2021-11-18 | 주식회사 대웅제약 | 신규한 헤테로사이클릭아민 유도체 및 이를 포함하는 약학 조성물 |
| MX2021003064A (es) * | 2018-09-18 | 2021-05-27 | Beijing Innocare Pharma Tech Co Ltd | Formas cristalinas de 6-(1-acriloilpiperidin-4-il)-2-(4-fenoxifeni l)nicotinamida. |
| MX2021004965A (es) * | 2018-11-06 | 2021-06-15 | Beijing Innocare Pharma Tech Co Ltd | Dispersion solida amorfa que comprende 6-(1-acriloilpiperidin-4-il )-2-(4-fenoxifenil)nicotinamida. |
| WO2020102304A1 (en) * | 2018-11-13 | 2020-05-22 | Rain Therapeutics Inc. | Combination of a kinase inhibitor and an electrolyte, compositions and methods comprising the same |
| PL3666262T3 (pl) * | 2018-12-10 | 2022-02-28 | Aphaia Ip Ag | Farmaceutyczne doustne postaci dawkowania do leczenia zaburzeń metabolicznych i powiązanych chorób poprzez zorganizowane uwalnianie enterokin |
| CN109851725A (zh) * | 2018-12-29 | 2019-06-07 | 华南理工大学 | 纳米纤维素-聚丙烯酰胺-明胶复合水凝胶、其制备方法及应用 |
| WO2020249001A1 (zh) | 2019-06-10 | 2020-12-17 | 百济神州瑞士有限责任公司 | 一种含有布鲁顿氏酪氨酸激酶抑制剂的口服固体片剂及其制备方法 |
| CN114787150A (zh) | 2019-08-15 | 2022-07-22 | 黑钻治疗公司 | 炔基喹唑啉化合物 |
| MX2022004427A (es) | 2019-10-14 | 2022-07-12 | Principia Biopharma Inc | Metodos para el tratamiento de la trombocitopenia inmunitaria mediante la administracion de (r)-2-[3-[4-amino-3-(2-fluoro-4-feno xi-fenil)pirazolo[3,4-d]pirimidin-1-il]piperidino-1-carbonil]-4-m etil-4-[4-(oxetan-3-il)piperazin-1-il]pent-2-enonitrilo. |
| WO2021080375A1 (en) * | 2019-10-24 | 2021-04-29 | Hanmi Pharm. Co., Ltd. | A pharmaceutical preparation comprising an amide derivative inhibiting the growth of cancer cell and a pharmaceutical product containing the same |
| KR20220130184A (ko) | 2020-01-22 | 2022-09-26 | 프린시피아 바이오파마, 인코퍼레이티드 | 2-[3-[4-아미노-3-(2-플루오로-4-페녹시-페닐)-1H-피라졸로[3,4-d]피리미딘-1-일]피페리딘-1-카르보닐]-4-메틸-4-[4-(옥세탄-3-일)피페라진-1-일]펜트-2-엔니트릴의 결정질 형태 |
| TW202235083A (zh) * | 2020-11-02 | 2022-09-16 | 美商黑鑽醫療公司 | 使用經炔取代之喹唑啉衍生物類以治療癌症之方法 |
| WO2022260667A1 (en) * | 2021-06-10 | 2022-12-15 | Hikma Pharmaceuticals Usa Inc. | Oral dosage forms of ibrutinib |
| CN113855695B (zh) * | 2021-11-01 | 2023-06-06 | 上海理工大学 | 一种结肠释药口服复方药物组合物及其制备方法 |
| CN114181159B (zh) * | 2021-12-28 | 2024-02-20 | 南通大学 | 含2,4,5-三取代嘧啶酰肼衍生物及其制备方法与应用 |
| US11786531B1 (en) | 2022-06-08 | 2023-10-17 | Beigene Switzerland Gmbh | Methods of treating B-cell proliferative disorder |
| CN116473923B (zh) * | 2023-05-29 | 2024-05-14 | 杭州剂泰医药科技有限责任公司 | 一种奈拉替尼固体分散体组合物及其制备方法和应用 |
Family Cites Families (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP2771010A4 (en) * | 2011-10-19 | 2015-04-01 | Pharmacyclics Inc | USE OF BRUTON TYROSINE KINASE (BTK) INHIBITORS |
| US20160045503A1 (en) * | 2012-06-18 | 2016-02-18 | Principia Biopharma Inc. | Formulations containing reversible covalent compounds |
| WO2014004707A1 (en) | 2012-06-29 | 2014-01-03 | Principia Biopharma Inc. | Formulations comprising ibrutinib |
| PL2892900T3 (pl) * | 2012-09-10 | 2018-02-28 | Principia Biopharma Inc. | Związki pyrazolopirymidonowe jako inhibitory kinazy |
| SG10201705437SA (en) * | 2013-01-05 | 2017-07-28 | Elcelyx Therapeutics Inc | Delayed-release composition comprising biguanide |
-
2015
- 2015-12-23 WO PCT/US2015/000515 patent/WO2016105582A1/en not_active Ceased
- 2015-12-23 US US15/539,100 patent/US20180193274A1/en not_active Abandoned
- 2015-12-23 MA MA41265A patent/MA41265B1/fr unknown
- 2015-12-23 EP EP15834774.0A patent/EP3236943B1/en active Active
- 2015-12-23 SI SI201531939T patent/SI3236943T1/sl unknown
- 2015-12-23 JP JP2017533932A patent/JP6687248B2/ja active Active
- 2015-12-23 LT LTEPPCT/US2015/000515T patent/LT3236943T/lt unknown
- 2015-12-23 HU HUE15834774A patent/HUE061809T2/hu unknown
- 2015-12-23 ES ES15834774T patent/ES2942642T3/es active Active
- 2015-12-23 PT PT158347740T patent/PT3236943T/pt unknown
- 2015-12-23 DK DK15834774.0T patent/DK3236943T3/da active
- 2015-12-23 RS RS20230281A patent/RS64139B1/sr unknown
- 2015-12-23 PL PL15834774.0T patent/PL3236943T3/pl unknown
- 2015-12-23 HR HRP20230305TT patent/HRP20230305T1/hr unknown
- 2015-12-23 FI FIEP15834774.0T patent/FI3236943T3/fi active
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