JP2018512413A5 - - Google Patents
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- Publication number
- JP2018512413A5 JP2018512413A5 JP2017549326A JP2017549326A JP2018512413A5 JP 2018512413 A5 JP2018512413 A5 JP 2018512413A5 JP 2017549326 A JP2017549326 A JP 2017549326A JP 2017549326 A JP2017549326 A JP 2017549326A JP 2018512413 A5 JP2018512413 A5 JP 2018512413A5
- Authority
- JP
- Japan
- Prior art keywords
- compound
- pharmaceutically acceptable
- acceptable salt
- inhibitor
- use according
- 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
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- 150000003839 salts Chemical class 0.000 claims 25
- 229940124291 BTK inhibitor Drugs 0.000 claims 11
- 150000001875 compounds Chemical class 0.000 claims 11
- 229940123729 mTOR kinase inhibitor Drugs 0.000 claims 11
- 239000003628 mammalian target of rapamycin inhibitor Substances 0.000 claims 11
- HKVAMNSJSFKALM-GKUWKFKPSA-N Everolimus Chemical compound C1C[C@@H](OCCO)[C@H](OC)C[C@@H]1C[C@@H](C)[C@H]1OC(=O)[C@@H]2CCCCN2C(=O)C(=O)[C@](O)(O2)[C@H](C)CC[C@H]2C[C@H](OC)/C(C)=C/C=C/C=C/[C@@H](C)C[C@@H](C)C(=O)[C@H](OC)[C@H](O)/C(C)=C/[C@@H](C)C(=O)C1 HKVAMNSJSFKALM-GKUWKFKPSA-N 0.000 claims 8
- 102000013530 TOR Serine-Threonine Kinases Human genes 0.000 claims 8
- 108010065917 TOR Serine-Threonine Kinases Proteins 0.000 claims 8
- 229940126214 compound 3 Drugs 0.000 claims 8
- 239000003814 drug Substances 0.000 claims 8
- 229960005167 everolimus Drugs 0.000 claims 8
- 239000008194 pharmaceutical composition Substances 0.000 claims 8
- 239000012664 BCL-2-inhibitor Substances 0.000 claims 6
- 239000002177 L01XE27 - Ibrutinib Substances 0.000 claims 6
- 229940125898 compound 5 Drugs 0.000 claims 6
- XYFPWWZEPKGCCK-GOSISDBHSA-N ibrutinib Chemical group C1=2C(N)=NC=NC=2N([C@H]2CN(CCC2)C(=O)C=C)N=C1C(C=C1)=CC=C1OC1=CC=CC=C1 XYFPWWZEPKGCCK-GOSISDBHSA-N 0.000 claims 6
- 229960001507 ibrutinib Drugs 0.000 claims 6
- ZAHRKKWIAAJSAO-UHFFFAOYSA-N rapamycin Natural products COCC(O)C(=C/C(C)C(=O)CC(OC(=O)C1CCCCN1C(=O)C(=O)C2(O)OC(CC(OC)C(=CC=CC=CC(C)CC(C)C(=O)C)C)CCC2C)C(C)CC3CCC(O)C(C3)OC)C ZAHRKKWIAAJSAO-UHFFFAOYSA-N 0.000 claims 6
- 229960002930 sirolimus Drugs 0.000 claims 6
- QFJCIRLUMZQUOT-HPLJOQBZSA-N sirolimus Chemical compound C1C[C@@H](O)[C@H](OC)C[C@@H]1C[C@@H](C)[C@H]1OC(=O)[C@@H]2CCCCN2C(=O)C(=O)[C@](O)(O2)[C@H](C)CC[C@H]2C[C@H](OC)/C(C)=C/C=C/C=C/[C@@H](C)C[C@@H](C)C(=O)[C@H](OC)[C@H](O)/C(C)=C/[C@@H](C)C(=O)C1 QFJCIRLUMZQUOT-HPLJOQBZSA-N 0.000 claims 6
- 229940123711 Bcl2 inhibitor Drugs 0.000 claims 5
- 206010028980 Neoplasm Diseases 0.000 claims 5
- 102000004022 Protein-Tyrosine Kinases Human genes 0.000 claims 4
- 108090000412 Protein-Tyrosine Kinases Proteins 0.000 claims 4
- 239000003112 inhibitor Substances 0.000 claims 4
- 229940043355 kinase inhibitor Drugs 0.000 claims 4
- 239000003757 phosphotransferase inhibitor Substances 0.000 claims 4
- 229960000688 pomalidomide Drugs 0.000 claims 4
- UVSMNLNDYGZFPF-UHFFFAOYSA-N pomalidomide Chemical compound O=C1C=2C(N)=CC=CC=2C(=O)N1C1CCC(=O)NC1=O UVSMNLNDYGZFPF-UHFFFAOYSA-N 0.000 claims 4
- LQBVNQSMGBZMKD-UHFFFAOYSA-N venetoclax Chemical group C=1C=C(Cl)C=CC=1C=1CC(C)(C)CCC=1CN(CC1)CCN1C(C=C1OC=2C=C3C=CNC3=NC=2)=CC=C1C(=O)NS(=O)(=O)C(C=C1[N+]([O-])=O)=CC=C1NCC1CCOCC1 LQBVNQSMGBZMKD-UHFFFAOYSA-N 0.000 claims 4
- 229960001183 venetoclax Drugs 0.000 claims 4
- VADOZMZXXRBXNY-UHFFFAOYSA-N 8-cyclopentyl-2-[4-(4-methylpiperazin-1-yl)anilino]-7-oxopyrido[2,3-d]pyrimidine-6-carbonitrile Chemical compound C1CN(C)CCN1C(C=C1)=CC=C1NC1=NC=C(C=C(C#N)C(=O)N2C3CCCC3)C2=N1 VADOZMZXXRBXNY-UHFFFAOYSA-N 0.000 claims 3
- 208000010839 B-cell chronic lymphocytic leukemia Diseases 0.000 claims 3
- 210000003719 b-lymphocyte Anatomy 0.000 claims 3
- 229940125904 compound 1 Drugs 0.000 claims 3
- 229940125782 compound 2 Drugs 0.000 claims 3
- 230000036210 malignancy Effects 0.000 claims 3
- 238000004519 manufacturing process Methods 0.000 claims 3
- 239000000203 mixture Substances 0.000 claims 3
- UEJJHQNACJXSKW-UHFFFAOYSA-N 2-(2,6-dioxopiperidin-3-yl)-1H-isoindole-1,3(2H)-dione Chemical compound O=C1C2=CC=CC=C2C(=O)N1C1CCC(=O)NC1=O UEJJHQNACJXSKW-UHFFFAOYSA-N 0.000 claims 2
- 208000023275 Autoimmune disease Diseases 0.000 claims 2
- 208000031671 Large B-Cell Diffuse Lymphoma Diseases 0.000 claims 2
- 208000031422 Lymphocytic Chronic B-Cell Leukemia Diseases 0.000 claims 2
- 208000025205 Mantle-Cell Lymphoma Diseases 0.000 claims 2
- 206010035226 Plasma cell myeloma Diseases 0.000 claims 2
- 201000011510 cancer Diseases 0.000 claims 2
- 206010012818 diffuse large B-cell lymphoma Diseases 0.000 claims 2
- 239000002955 immunomodulating agent Substances 0.000 claims 2
- 229940121354 immunomodulator Drugs 0.000 claims 2
- 230000002584 immunomodulator Effects 0.000 claims 2
- 229960004942 lenalidomide Drugs 0.000 claims 2
- GOTYRUGSSMKFNF-UHFFFAOYSA-N lenalidomide Chemical compound C1C=2C(N)=CC=CC=2C(=O)N1C1CCC(=O)NC1=O GOTYRUGSSMKFNF-UHFFFAOYSA-N 0.000 claims 2
- 229960003433 thalidomide Drugs 0.000 claims 2
- VVHQVXXPZDALDV-BOXHHOBZSA-N (3s)-3-[7-[[4-(morpholin-4-ylmethyl)phenyl]methoxy]-3-oxo-1h-isoindol-2-yl]piperidine-2,6-dione;hydrochloride Chemical compound Cl.O=C1N([C@@H]2C(NC(=O)CC2)=O)CC2=C1C=CC=C2OCC(C=C1)=CC=C1CN1CCOCC1 VVHQVXXPZDALDV-BOXHHOBZSA-N 0.000 claims 1
- RSNPAKAFCAAMBH-UHFFFAOYSA-N 3-(5-amino-2-methyl-4-oxoquinazolin-3-yl)piperidine-2,6-dione Chemical compound CC1=NC2=CC=CC(N)=C2C(=O)N1C1CCC(=O)NC1=O RSNPAKAFCAAMBH-UHFFFAOYSA-N 0.000 claims 1
- 229940045793 B-cell lymphoma-2 inhibitor Drugs 0.000 claims 1
- 206010009900 Colitis ulcerative Diseases 0.000 claims 1
- 206010025323 Lymphomas Diseases 0.000 claims 1
- 208000034578 Multiple myelomas Diseases 0.000 claims 1
- 201000004681 Psoriasis Diseases 0.000 claims 1
- 201000006704 Ulcerative Colitis Diseases 0.000 claims 1
- 208000016025 Waldenstroem macroglobulinemia Diseases 0.000 claims 1
- 208000033559 Waldenström macroglobulinemia Diseases 0.000 claims 1
- 208000010928 autoimmune thyroid disease Diseases 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 201000003444 follicular lymphoma Diseases 0.000 claims 1
- 208000026278 immune system disease Diseases 0.000 claims 1
- 201000006417 multiple sclerosis Diseases 0.000 claims 1
- 201000000050 myeloid neoplasm Diseases 0.000 claims 1
- 206010039073 rheumatoid arthritis Diseases 0.000 claims 1
- 201000000596 systemic lupus erythematosus Diseases 0.000 claims 1
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP2021173052A JP2022003103A (ja) | 2015-03-19 | 2021-10-22 | 癌および自己免疫疾患を治療するための最適化された組合せ療法およびその使用 |
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201510119944.5 | 2015-03-19 | ||
| CN201510119944.5A CN106146508A (zh) | 2015-03-19 | 2015-03-19 | 优化的联合用药及其治疗癌症和自身免疫疾病的用途 |
| PCT/CN2016/000149 WO2016145935A1 (zh) | 2015-03-19 | 2016-03-18 | 优化的联合用药及其治疗癌症和自身免疫疾病的用途 |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2021173052A Division JP2022003103A (ja) | 2015-03-19 | 2021-10-22 | 癌および自己免疫疾患を治療するための最適化された組合せ療法およびその使用 |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2018512413A JP2018512413A (ja) | 2018-05-17 |
| JP2018512413A5 true JP2018512413A5 (enExample) | 2019-04-04 |
| JP7012534B2 JP7012534B2 (ja) | 2022-02-14 |
Family
ID=56918303
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2017549326A Active JP7012534B2 (ja) | 2015-03-19 | 2016-03-18 | 癌および自己免疫疾患を治療するための最適化された組合せ療法およびその使用 |
| JP2021173052A Pending JP2022003103A (ja) | 2015-03-19 | 2021-10-22 | 癌および自己免疫疾患を治療するための最適化された組合せ療法およびその使用 |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2021173052A Pending JP2022003103A (ja) | 2015-03-19 | 2021-10-22 | 癌および自己免疫疾患を治療するための最適化された組合せ療法およびその使用 |
Country Status (11)
| Country | Link |
|---|---|
| EP (1) | EP3272752A4 (enExample) |
| JP (2) | JP7012534B2 (enExample) |
| KR (2) | KR20220110872A (enExample) |
| CN (4) | CN106146508A (enExample) |
| AU (2) | AU2016232923B2 (enExample) |
| BR (1) | BR112017019790B1 (enExample) |
| CA (2) | CA3191171A1 (enExample) |
| EA (2) | EA202092671A1 (enExample) |
| IL (1) | IL254435B2 (enExample) |
| MX (1) | MX2017011836A (enExample) |
| WO (1) | WO2016145935A1 (enExample) |
Families Citing this family (27)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN105017256A (zh) * | 2014-04-29 | 2015-11-04 | 浙江导明医药科技有限公司 | 多氟化合物作为布鲁顿酪氨酸激酶抑制剂 |
| CN106146508A (zh) * | 2015-03-19 | 2016-11-23 | 浙江导明医药科技有限公司 | 优化的联合用药及其治疗癌症和自身免疫疾病的用途 |
| US9717745B2 (en) * | 2015-03-19 | 2017-08-01 | Zhejiang DTRM Biopharma Co. Ltd. | Pharmaceutical compositions and their use for treatment of cancer and autoimmune diseases |
| US10711006B2 (en) | 2016-11-15 | 2020-07-14 | Hangzhou Hertz Pharmaceutical Co., Ltd. | Selective Bruton's tyrosine kinase inhibitor and use thereof |
| CN106831788B (zh) * | 2017-01-22 | 2020-10-30 | 鲁南制药集团股份有限公司 | 伊布替尼精制方法 |
| KR20200032751A (ko) * | 2017-09-15 | 2020-03-26 | 아두로 바이오테크, 인코포레이티드 | 피라졸로피리미디논 화합물 및 그의 용도 |
| TW201922256A (zh) * | 2017-10-27 | 2019-06-16 | 中國大陸商浙江導明醫藥科技有限公司 | 治療淋巴樣惡性疾病之方法 |
| WO2019127008A1 (zh) * | 2017-12-26 | 2019-07-04 | 清华大学 | 一种靶向降解btk的化合物及其应用 |
| CA3085457C (en) | 2018-01-29 | 2023-05-23 | Dana-Farber Cancer Institute, Inc. | Degradation of bruton's tyrosine kinase (btk) by conjugation of btk inhibitors with e3 ligase ligand and methods of use |
| GB201809746D0 (en) * | 2018-06-14 | 2018-08-01 | Berlin Chemie Ag | Pharmaceutical combinations |
| CN108992454B (zh) * | 2018-06-20 | 2020-06-02 | 合肥医工医药股份有限公司 | 一种治疗皮肤炎症性疾病的复方药物组合物 |
| CN114522167A (zh) * | 2018-07-31 | 2022-05-24 | 苏州亚盛药业有限公司 | Bcl-2抑制剂或Bcl-2/Bcl-xL抑制剂与BTK抑制剂的组合产品及其用途 |
| CN109369654A (zh) * | 2018-11-20 | 2019-02-22 | 山东大学 | 1，3-二取代-4-氨基吡唑并嘧啶类化合物及其制备方法和应用 |
| KR102819183B1 (ko) * | 2019-03-29 | 2025-06-13 | 한미약품 주식회사 | 퓨로피리미딘 화합물의 산 부가염의 결정형 |
| WO2021064142A1 (en) | 2019-10-02 | 2021-04-08 | Tolremo Therapeutics Ag | Heterocyclic derivatives, pharmaceutical compositions and their use in the treatment or amelioration of cancer |
| CN110724143B (zh) * | 2019-10-09 | 2021-03-23 | 清华大学 | 一种靶向btk蛋白降解化合物的制备及其在治疗自身免疫系统疾病与肿瘤中的应用 |
| CN110845500B (zh) * | 2019-10-09 | 2021-05-11 | 清华大学 | 靶向btk降解化合物在治疗自身免疫系统疾病中的应用 |
| CN115701996B (zh) * | 2020-06-25 | 2024-12-24 | 托雷莫治疗股份公司 | 用于治疗EGFR突变型NSCLC的CBP/p300溴结构域抑制剂和EGFR抑制剂的组合 |
| CA3184076A1 (en) | 2020-06-25 | 2021-12-30 | Stefanie Fluckiger-Mangual | Combination of a cbp/p300 bromodomain inhibitor and a kras inhibitor for the treatment of cancer |
| CN113943312A (zh) * | 2020-07-17 | 2022-01-18 | 轶诺(浙江)药业有限公司 | 一类肠道裂解型共药及其制备和用途 |
| MA61557B1 (fr) * | 2020-09-17 | 2025-05-30 | Novartis Ag | Composés et compositions servant d'inhibiteurs de sppl2a |
| WO2022097136A1 (en) * | 2020-11-04 | 2022-05-12 | Immune System Key Ltd. | Polypeptides for use in the treatment and prevention of neurodegenerative diseases |
| CN114507236A (zh) * | 2022-02-28 | 2022-05-17 | 山东中医药大学 | mTOR蛋白降解靶向嵌合体及其制备方法和应用 |
| WO2023197914A1 (zh) * | 2022-04-12 | 2023-10-19 | 安徽中科拓苒药物科学研究有限公司 | 一种吡唑并嘧啶类化合物的新用途 |
| CN117045800A (zh) * | 2022-05-06 | 2023-11-14 | 上海科技大学 | mTOR抑制剂增强靶向蛋白降解药物功效的应用 |
| CN116024346A (zh) * | 2023-02-10 | 2023-04-28 | 复旦大学附属华山医院 | SLCO1B1 rs2306283位点多态性在评价甲氨蝶呤所致骨髓抑制发生风险中的应用 |
| CN117510494B (zh) * | 2023-11-07 | 2024-04-19 | 桂林医学院附属医院 | β-咔啉-沙利度胺偶联物及其在制备逆转ABT-199耐药的药物中的应用 |
Family Cites Families (18)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| SI2529622T1 (en) * | 2006-09-22 | 2018-06-29 | Pharmacyclics Llc | Inhibitors of bruton's tyrosine kinase |
| EP1921149A1 (en) * | 2006-11-13 | 2008-05-14 | AEterna Zentaris GmbH | Microorganisms as carriers of nucleotide sequences coding for antigens and protein toxins, process of manufacturing and uses thereof |
| SG10201508035TA (en) * | 2007-03-28 | 2015-10-29 | Pharmacyclics Inc | Inhibitors of bruton's tyrosine kinase |
| WO2010009342A2 (en) * | 2008-07-16 | 2010-01-21 | Pharmacyclics, Inc. | Inhibitors of bruton's tyrosine kinase for the treatment of solid tumors |
| US7741330B1 (en) * | 2009-10-12 | 2010-06-22 | Pharmacyclics, Inc. | Pyrazolo-pyrimidine inhibitors of Bruton's tyrosine kinase |
| BR112013028846B1 (pt) | 2011-05-17 | 2021-12-07 | Principia Biopharma Inc | Composto ou sal farmaceuticamente aceitável do mesmo, respectivos usos, processo de preparação, intermediários e composição farmacêutica |
| KR20140048968A (ko) | 2011-07-13 | 2014-04-24 | 파마시클릭스, 인코포레이티드 | 브루톤형 티로신 키나제의 억제제 |
| WO2013191965A1 (en) | 2012-06-18 | 2013-12-27 | Principia Biopharma Inc. | Reversible covalent pyrrolo- or pyrazolopyrimidines useful for the treatment cancer and autoimmune diseases |
| BR112015001839A2 (pt) | 2012-07-30 | 2017-07-04 | Concert Pharmaceuticals Inc | ibrutinibe deuterado |
| WO2014022569A1 (en) | 2012-08-03 | 2014-02-06 | Principia Biopharma Inc. | Treatment of dry eye |
| NZ708563A (en) | 2012-11-01 | 2019-02-22 | Infinity Pharmaceuticals Inc | Treatment of cancers using pi3 kinase isoform modulators |
| WO2014113942A1 (en) * | 2013-01-23 | 2014-07-31 | Merck Sharp & Dohme Corp. | Btk inhibitors |
| WO2014143807A2 (en) * | 2013-03-15 | 2014-09-18 | Stromatt Scott | Anti-cd37 antibody and bcr pathway antagonist combination therapy for treatment of b-cell malignancies and disorders |
| US8957080B2 (en) * | 2013-04-09 | 2015-02-17 | Principia Biopharma Inc. | Tyrosine kinase inhibitors |
| BR112015026006B1 (pt) * | 2013-04-17 | 2022-10-18 | Signal Pharmaceuticals, Llc | Uso de um composto em combinação com um fármaco imunomodulador imid® para tratamento ou prevenção de um câncer, composição farmacêutica e kit compreendendo os referidos compostos |
| WO2014187319A1 (en) * | 2013-05-21 | 2014-11-27 | Jiangsu Medolution Ltd | Substituted pyrazolopyrimidines as kinases inhibitors |
| CN105017256A (zh) * | 2014-04-29 | 2015-11-04 | 浙江导明医药科技有限公司 | 多氟化合物作为布鲁顿酪氨酸激酶抑制剂 |
| CN106146508A (zh) * | 2015-03-19 | 2016-11-23 | 浙江导明医药科技有限公司 | 优化的联合用药及其治疗癌症和自身免疫疾病的用途 |
-
2015
- 2015-03-19 CN CN201510119944.5A patent/CN106146508A/zh active Pending
-
2016
- 2016-03-18 JP JP2017549326A patent/JP7012534B2/ja active Active
- 2016-03-18 BR BR112017019790-1A patent/BR112017019790B1/pt active IP Right Grant
- 2016-03-18 CN CN202111303221.2A patent/CN114790209A/zh active Pending
- 2016-03-18 EP EP16764117.4A patent/EP3272752A4/en active Pending
- 2016-03-18 KR KR1020227026364A patent/KR20220110872A/ko not_active Ceased
- 2016-03-18 KR KR1020177025465A patent/KR102428387B1/ko active Active
- 2016-03-18 EA EA202092671A patent/EA202092671A1/ru unknown
- 2016-03-18 WO PCT/CN2016/000149 patent/WO2016145935A1/zh not_active Ceased
- 2016-03-18 CN CN201680017009.0A patent/CN107406454B/zh active Active
- 2016-03-18 CA CA3191171A patent/CA3191171A1/en active Pending
- 2016-03-18 CA CA2980016A patent/CA2980016C/en active Active
- 2016-03-18 IL IL254435A patent/IL254435B2/en unknown
- 2016-03-18 CN CN202010319886.1A patent/CN111349099A/zh active Pending
- 2016-03-18 AU AU2016232923A patent/AU2016232923B2/en active Active
- 2016-03-18 MX MX2017011836A patent/MX2017011836A/es unknown
- 2016-03-18 EA EA201792066A patent/EA037058B1/ru unknown
-
2020
- 2020-11-24 AU AU2020277128A patent/AU2020277128B2/en active Active
-
2021
- 2021-10-22 JP JP2021173052A patent/JP2022003103A/ja active Pending
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