JP2020040989A5 - - Google Patents
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- JP2020040989A5 JP2020040989A5 JP2019220363A JP2019220363A JP2020040989A5 JP 2020040989 A5 JP2020040989 A5 JP 2020040989A5 JP 2019220363 A JP2019220363 A JP 2019220363A JP 2019220363 A JP2019220363 A JP 2019220363A JP 2020040989 A5 JP2020040989 A5 JP 2020040989A5
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- JP
- Japan
- Prior art keywords
- pharmaceutically acceptable
- compound
- acceptable salt
- enantiomer
- diastereomer
- 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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- 150000003839 salts Chemical class 0.000 claims 18
- 150000001875 compounds Chemical class 0.000 claims 17
- 102000001714 Agammaglobulinaemia Tyrosine Kinase Human genes 0.000 claims 7
- 108010029445 Agammaglobulinaemia Tyrosine Kinase Proteins 0.000 claims 7
- 208000010839 B-cell chronic lymphocytic leukemia Diseases 0.000 claims 6
- 239000008194 pharmaceutical composition Substances 0.000 claims 6
- -1 CF 3 Inorganic materials 0.000 claims 5
- 208000023275 Autoimmune disease Diseases 0.000 claims 4
- YZCKVEUIGOORGS-OUBTZVSYSA-N Deuterium Chemical compound [2H] YZCKVEUIGOORGS-OUBTZVSYSA-N 0.000 claims 4
- 208000031671 Large B-Cell Diffuse Lymphoma Diseases 0.000 claims 4
- 208000031422 Lymphocytic Chronic B-Cell Leukemia Diseases 0.000 claims 4
- 208000025205 Mantle-Cell Lymphoma Diseases 0.000 claims 4
- 206010028980 Neoplasm Diseases 0.000 claims 4
- 208000016025 Waldenstroem macroglobulinemia Diseases 0.000 claims 4
- 208000033559 Waldenström macroglobulinemia Diseases 0.000 claims 4
- 210000003719 b-lymphocyte Anatomy 0.000 claims 4
- 229910052805 deuterium Inorganic materials 0.000 claims 4
- 206010012818 diffuse large B-cell lymphoma Diseases 0.000 claims 4
- 230000000694 effects Effects 0.000 claims 4
- 201000003444 follicular lymphoma Diseases 0.000 claims 4
- 230000036210 malignancy Effects 0.000 claims 4
- 125000000391 vinyl group Chemical group [H]C([*])=C([H])[H] 0.000 claims 4
- 229920002554 vinyl polymer Polymers 0.000 claims 4
- 125000000753 cycloalkyl group Chemical group 0.000 claims 3
- 239000003814 drug Substances 0.000 claims 3
- 238000004519 manufacturing process Methods 0.000 claims 3
- 125000000882 C2-C6 alkenyl group Chemical group 0.000 claims 2
- 206010009900 Colitis ulcerative Diseases 0.000 claims 2
- 208000034578 Multiple myelomas Diseases 0.000 claims 2
- 206010035226 Plasma cell myeloma Diseases 0.000 claims 2
- CZPWVGJYEJSRLH-UHFFFAOYSA-N Pyrimidine Chemical compound C1=CN=CN=C1 CZPWVGJYEJSRLH-UHFFFAOYSA-N 0.000 claims 2
- 208000034189 Sclerosis Diseases 0.000 claims 2
- 201000006704 Ulcerative Colitis Diseases 0.000 claims 2
- 125000002252 acyl group Chemical group 0.000 claims 2
- 125000003368 amide group Chemical group 0.000 claims 2
- 230000002490 cerebral effect Effects 0.000 claims 2
- 230000002401 inhibitory effect Effects 0.000 claims 2
- 230000005764 inhibitory process Effects 0.000 claims 2
- 125000003386 piperidinyl group Chemical group 0.000 claims 2
- 125000000719 pyrrolidinyl group Chemical group 0.000 claims 2
- LISFMEBWQUVKPJ-UHFFFAOYSA-N quinolin-2-ol Chemical compound C1=CC=C2NC(=O)C=CC2=C1 LISFMEBWQUVKPJ-UHFFFAOYSA-N 0.000 claims 2
- 206010039073 rheumatoid arthritis Diseases 0.000 claims 2
- 201000000596 systemic lupus erythematosus Diseases 0.000 claims 2
- 125000004044 trifluoroacetyl group Chemical group FC(C(=O)*)(F)F 0.000 claims 2
- 125000000876 trifluoromethoxy group Chemical group FC(F)(F)O* 0.000 claims 2
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 claims 2
- DFLMYGVQULGUFP-OAHLLOKOSA-N 1-[(3R)-3-[4-amino-3-[2-fluoro-4-(2-fluorobenzoyl)phenyl]pyrazolo[3,4-d]pyrimidin-1-yl]pyrrolidin-1-yl]prop-2-en-1-one Chemical compound NC1=C2C(=NC=N1)N(N=C2C1=C(C=C(C=C1)C(C1=C(C=CC=C1)F)=O)F)[C@H]1CN(CC1)C(C=C)=O DFLMYGVQULGUFP-OAHLLOKOSA-N 0.000 claims 1
- HBAQYPYDRFILMT-UHFFFAOYSA-N 8-[3-(1-cyclopropylpyrazol-4-yl)-1H-pyrazolo[4,3-d]pyrimidin-5-yl]-3-methyl-3,8-diazabicyclo[3.2.1]octan-2-one Chemical class C1(CC1)N1N=CC(=C1)C1=NNC2=C1N=C(N=C2)N1C2C(N(CC1CC2)C)=O HBAQYPYDRFILMT-UHFFFAOYSA-N 0.000 claims 1
- HRPVXLWXLXDGHG-UHFFFAOYSA-N Acrylamide Chemical compound NC(=O)C=C HRPVXLWXLXDGHG-UHFFFAOYSA-N 0.000 claims 1
- 125000003601 C2-C6 alkynyl group Chemical group 0.000 claims 1
- QKBXFLHSJNQHKV-LLVKDONJSA-N FC1=C(C=CC(=C1)OC1=C(C(=CC(=C1F)F)F)F)C1=NN(C2=NC=NC(=C21)N)[C@H]1CN(CC1)S(=O)(=O)C=C Chemical compound FC1=C(C=CC(=C1)OC1=C(C(=CC(=C1F)F)F)F)C1=NN(C2=NC=NC(=C21)N)[C@H]1CN(CC1)S(=O)(=O)C=C QKBXFLHSJNQHKV-LLVKDONJSA-N 0.000 claims 1
- OAKJQQAXSVQMHS-UHFFFAOYSA-N Hydrazine Chemical group NN OAKJQQAXSVQMHS-UHFFFAOYSA-N 0.000 claims 1
- ZJDIFXCDJKKPIO-UHFFFAOYSA-N NC1=C2C(=NC=N1)N(N=C2C1=C(C=C(C=C1)OC1=C(C(=CC(=C1F)F)F)F)F)C1CN(CC1)C(C=C)=O Chemical compound NC1=C2C(=NC=N1)N(N=C2C1=C(C=C(C=C1)OC1=C(C(=CC(=C1F)F)F)F)F)C1CN(CC1)C(C=C)=O ZJDIFXCDJKKPIO-UHFFFAOYSA-N 0.000 claims 1
- QLRDEQPODCORHJ-UHFFFAOYSA-N NC1=C2C(=NC=N1)N(N=C2C1=C(C=C(C=C1)OC1=CC(=CC=C1)F)F)C1CN(CC1)C(C=C)=O Chemical compound NC1=C2C(=NC=N1)N(N=C2C1=C(C=C(C=C1)OC1=CC(=CC=C1)F)F)C1CN(CC1)C(C=C)=O QLRDEQPODCORHJ-UHFFFAOYSA-N 0.000 claims 1
- 125000003545 alkoxy group Chemical group 0.000 claims 1
- 125000000217 alkyl group Chemical group 0.000 claims 1
- 125000003118 aryl group Chemical group 0.000 claims 1
- 201000011510 cancer Diseases 0.000 claims 1
- 125000002915 carbonyl group Chemical group [*:2]C([*:1])=O 0.000 claims 1
- 125000004093 cyano group Chemical group *C#N 0.000 claims 1
- 125000000113 cyclohexyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])(*)C([H])([H])C1([H])[H] 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 125000004185 ester group Chemical group 0.000 claims 1
- 125000001207 fluorophenyl group Chemical group 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
- 125000000592 heterocycloalkyl group Chemical group 0.000 claims 1
- 229910052739 hydrogen Inorganic materials 0.000 claims 1
- 125000002768 hydroxyalkyl group Chemical group 0.000 claims 1
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 claims 1
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims 1
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201410175783.7 | 2014-04-29 | ||
| CN201410175783.7A CN105017256A (zh) | 2014-04-29 | 2014-04-29 | 多氟化合物作为布鲁顿酪氨酸激酶抑制剂 |
Related Parent Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2016565402A Division JP6670756B2 (ja) | 2014-04-29 | 2015-04-27 | ブルトン型チロシンキナーゼ（ｂｔｋ）インヒビターとしての多フルオロ置換化合物 |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2020040989A JP2020040989A (ja) | 2020-03-19 |
| JP2020040989A5 true JP2020040989A5 (https=) | 2020-07-09 |
| JP7005582B2 JP7005582B2 (ja) | 2022-01-21 |
Family
ID=54358137
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2016565402A Active JP6670756B2 (ja) | 2014-04-29 | 2015-04-27 | ブルトン型チロシンキナーゼ（ｂｔｋ）インヒビターとしての多フルオロ置換化合物 |
| JP2019220363A Active JP7005582B2 (ja) | 2014-04-29 | 2019-12-05 | ブルトン型チロシンキナーゼ（ｂｔｋ）インヒビターとしての多フルオロ置換化合物 |
Family Applications Before (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2016565402A Active JP6670756B2 (ja) | 2014-04-29 | 2015-04-27 | ブルトン型チロシンキナーゼ（ｂｔｋ）インヒビターとしての多フルオロ置換化合物 |
Country Status (13)
| Country | Link |
|---|---|
| US (3) | US9532990B2 (https=) |
| EP (1) | EP3138842B1 (https=) |
| JP (2) | JP6670756B2 (https=) |
| KR (2) | KR20160144378A (https=) |
| CN (3) | CN105017256A (https=) |
| AU (1) | AU2015252654C1 (https=) |
| BR (1) | BR112016025132A2 (https=) |
| CA (1) | CA2947338C (https=) |
| EA (2) | EA037227B1 (https=) |
| ES (1) | ES2857251T3 (https=) |
| IL (1) | IL248546B (https=) |
| MX (2) | MX387487B (https=) |
| WO (1) | WO2015165279A1 (https=) |
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| TR201907147T4 (tr) | 2013-07-18 | 2019-06-21 | Taiho Pharmaceutical Co Ltd | Fgfr inhibitörünün aralıklı uygulanmasına yönelik anti-tümör ilaç. |
| 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 |
| EP3221320A4 (en) * | 2014-11-19 | 2018-04-25 | Sun Pharmaceutical Industries Ltd | A process for the preparation of ibrutinib |
| US10214532B2 (en) | 2015-02-12 | 2019-02-26 | Shanghai Dude Medical Science and Technology Co., Ltd. | Process for preparing ibrutinib |
| 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 |
| CN106146511A (zh) * | 2015-04-03 | 2016-11-23 | 安润医药科技（苏州）有限公司 | 吡唑并嘧啶衍生物、制备方法、药物组合物及用途 |
| CN106146512B (zh) * | 2015-04-09 | 2018-07-17 | 北京睿创康泰医药研究院有限公司 | 依鲁替尼的制备方法 |
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| CN107501270B (zh) * | 2017-09-01 | 2019-06-28 | 宏腾建设集团有限公司 | 一种含有磺酰吖丙啶结构的化合物、药物组合物以及其应用 |
| 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 |
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| CN111454268B (zh) * | 2019-01-18 | 2023-09-08 | 明慧医药（上海）有限公司 | 作为布鲁顿酪氨酸激酶抑制剂的环状分子 |
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| US20220143049A1 (en) | 2019-03-21 | 2022-05-12 | Onxeo | A dbait molecule in combination with kinase inhibitor for the treatment of cancer |
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2014
- 2014-04-29 CN CN201410175783.7A patent/CN105017256A/zh active Pending
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2015
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- 2015-04-27 JP JP2016565402A patent/JP6670756B2/ja active Active
- 2015-04-27 AU AU2015252654A patent/AU2015252654C1/en active Active
- 2015-04-27 KR KR1020167028059A patent/KR20160144378A/ko not_active Ceased
- 2015-04-27 EA EA201692176A patent/EA032100B1/ru unknown
- 2015-04-27 ES ES15785217T patent/ES2857251T3/es active Active
- 2015-04-27 CN CN201580010345.8A patent/CN106061976B/zh active Active
- 2015-04-27 BR BR112016025132A patent/BR112016025132A2/pt not_active Application Discontinuation
- 2015-04-27 KR KR1020237032203A patent/KR102669966B1/ko active Active
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2016
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2017
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2019
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