JP2014520863A5 - - Google Patents
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- JP2014520863A5 JP2014520863A5 JP2014520391A JP2014520391A JP2014520863A5 JP 2014520863 A5 JP2014520863 A5 JP 2014520863A5 JP 2014520391 A JP2014520391 A JP 2014520391A JP 2014520391 A JP2014520391 A JP 2014520391A JP 2014520863 A5 JP2014520863 A5 JP 2014520863A5
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- Prior art keywords
- alkyl
- substituted
- unsubstituted
- cycloalkyl
- optionally substituted
- Prior art date
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- 150000001875 compounds Chemical class 0.000 claims 70
- 229910052799 carbon Inorganic materials 0.000 claims 46
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 claims 34
- 229910052739 hydrogen Inorganic materials 0.000 claims 34
- 125000006716 (C1-C6) heteroalkyl group Chemical group 0.000 claims 29
- 229910052736 halogen Inorganic materials 0.000 claims 28
- 150000002367 halogens Chemical class 0.000 claims 28
- 125000001072 heteroaryl group Chemical group 0.000 claims 23
- 229910052760 oxygen Inorganic materials 0.000 claims 21
- 229910052717 sulfur Inorganic materials 0.000 claims 21
- 150000001204 N-oxides Chemical class 0.000 claims 20
- 239000000651 prodrug Substances 0.000 claims 20
- 229940002612 prodrug Drugs 0.000 claims 20
- 150000003839 salts Chemical class 0.000 claims 20
- 239000012453 solvate Substances 0.000 claims 20
- 125000003118 aryl group Chemical group 0.000 claims 16
- 125000000592 heterocycloalkyl group Chemical group 0.000 claims 14
- 125000005346 substituted cycloalkyl group Chemical group 0.000 claims 10
- RWRDLPDLKQPQOW-UHFFFAOYSA-N Pyrrolidine Chemical compound C1CCNC1 RWRDLPDLKQPQOW-UHFFFAOYSA-N 0.000 claims 9
- 125000000217 alkyl group Chemical group 0.000 claims 9
- 125000000753 cycloalkyl group Chemical group 0.000 claims 7
- 125000003107 substituted aryl group Chemical group 0.000 claims 7
- NQRYJNQNLNOLGT-UHFFFAOYSA-N Piperidine Chemical compound C1CCNCC1 NQRYJNQNLNOLGT-UHFFFAOYSA-N 0.000 claims 6
- 125000000547 substituted alkyl group Chemical group 0.000 claims 6
- 239000003814 drug Substances 0.000 claims 5
- 239000000203 mixture Substances 0.000 claims 5
- JUJWROOIHBZHMG-UHFFFAOYSA-N Pyridine Chemical compound C1=CC=NC=C1 JUJWROOIHBZHMG-UHFFFAOYSA-N 0.000 claims 4
- 238000004519 manufacturing process Methods 0.000 claims 4
- 239000008194 pharmaceutical composition Substances 0.000 claims 4
- YLQBMQCUIZJEEH-UHFFFAOYSA-N Furan Chemical compound C=1C=COC=1 YLQBMQCUIZJEEH-UHFFFAOYSA-N 0.000 claims 3
- 125000005842 heteroatom Chemical group 0.000 claims 3
- 239000001257 hydrogen Substances 0.000 claims 3
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims 3
- RAXXELZNTBOGNW-UHFFFAOYSA-N imidazole Natural products C1=CNC=N1 RAXXELZNTBOGNW-UHFFFAOYSA-N 0.000 claims 3
- 208000031422 Lymphocytic Chronic B-Cell Leukemia Diseases 0.000 claims 2
- 206010028980 Neoplasm Diseases 0.000 claims 2
- ZCQWOFVYLHDMMC-UHFFFAOYSA-N Oxazole Chemical compound C1=COC=N1 ZCQWOFVYLHDMMC-UHFFFAOYSA-N 0.000 claims 2
- KYQCOXFCLRTKLS-UHFFFAOYSA-N Pyrazine Chemical compound C1=CN=CC=N1 KYQCOXFCLRTKLS-UHFFFAOYSA-N 0.000 claims 2
- WYURNTSHIVDZCO-UHFFFAOYSA-N Tetrahydrofuran Chemical compound C1CCOC1 WYURNTSHIVDZCO-UHFFFAOYSA-N 0.000 claims 2
- YTPLMLYBLZKORZ-UHFFFAOYSA-N Thiophene Chemical compound C=1C=CSC=1 YTPLMLYBLZKORZ-UHFFFAOYSA-N 0.000 claims 2
- 125000003545 alkoxy group Chemical group 0.000 claims 2
- 210000003719 b-lymphocyte Anatomy 0.000 claims 2
- 201000011510 cancer Diseases 0.000 claims 2
- 125000004093 cyano group Chemical group *C#N 0.000 claims 2
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 2
- 208000035475 disorder Diseases 0.000 claims 2
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 2
- 208000026278 immune system disease Diseases 0.000 claims 2
- CTAPFRYPJLPFDF-UHFFFAOYSA-N isoxazole Chemical compound C=1C=NOC=1 CTAPFRYPJLPFDF-UHFFFAOYSA-N 0.000 claims 2
- WCPAKWJPBJAGKN-UHFFFAOYSA-N oxadiazole Chemical compound C1=CON=N1 WCPAKWJPBJAGKN-UHFFFAOYSA-N 0.000 claims 2
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 2
- 230000002062 proliferating effect Effects 0.000 claims 2
- UMJSCPRVCHMLSP-UHFFFAOYSA-N pyridine Natural products COC1=CC=CN=C1 UMJSCPRVCHMLSP-UHFFFAOYSA-N 0.000 claims 2
- OIWIYLWZIIJNHU-UHFFFAOYSA-N 1-sulfanylpyrazole Chemical compound SN1C=CC=N1 OIWIYLWZIIJNHU-UHFFFAOYSA-N 0.000 claims 1
- 208000023275 Autoimmune disease Diseases 0.000 claims 1
- 208000010839 B-cell chronic lymphocytic leukemia Diseases 0.000 claims 1
- AVXURJPOCDRRFD-UHFFFAOYSA-N Hydroxylamine Chemical group ON AVXURJPOCDRRFD-UHFFFAOYSA-N 0.000 claims 1
- 208000031671 Large B-Cell Diffuse Lymphoma Diseases 0.000 claims 1
- 206010052178 Lymphocytic lymphoma Diseases 0.000 claims 1
- PCNDJXKNXGMECE-UHFFFAOYSA-N Phenazine Natural products C1=CC=CC2=NC3=CC=CC=C3N=C21 PCNDJXKNXGMECE-UHFFFAOYSA-N 0.000 claims 1
- WTKZEGDFNFYCGP-UHFFFAOYSA-N Pyrazole Chemical compound C=1C=NNC=1 WTKZEGDFNFYCGP-UHFFFAOYSA-N 0.000 claims 1
- CZPWVGJYEJSRLH-UHFFFAOYSA-N Pyrimidine Chemical compound C1=CN=CN=C1 CZPWVGJYEJSRLH-UHFFFAOYSA-N 0.000 claims 1
- DHXVGJBLRPWPCS-UHFFFAOYSA-N Tetrahydropyran Chemical compound C1CCOCC1 DHXVGJBLRPWPCS-UHFFFAOYSA-N 0.000 claims 1
- FZWLAAWBMGSTSO-UHFFFAOYSA-N Thiazole Chemical compound C1=CSC=N1 FZWLAAWBMGSTSO-UHFFFAOYSA-N 0.000 claims 1
- 125000004183 alkoxy alkyl group Chemical group 0.000 claims 1
- 125000004453 alkoxycarbonyl group Chemical group 0.000 claims 1
- 125000004448 alkyl carbonyl group Chemical group 0.000 claims 1
- 125000003710 aryl alkyl group Chemical group 0.000 claims 1
- 125000004429 atom Chemical group 0.000 claims 1
- 239000011230 binding agent Substances 0.000 claims 1
- 125000003917 carbamoyl group Chemical group [H]N([H])C(*)=O 0.000 claims 1
- 230000001684 chronic effect Effects 0.000 claims 1
- 208000032852 chronic lymphocytic leukemia Diseases 0.000 claims 1
- 206010012818 diffuse large B-cell lymphoma Diseases 0.000 claims 1
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims 1
- 201000003444 follicular lymphoma Diseases 0.000 claims 1
- 125000004404 heteroalkyl group Chemical group 0.000 claims 1
- 125000000623 heterocyclic group Chemical group 0.000 claims 1
- 125000002768 hydroxyalkyl group Chemical group 0.000 claims 1
- 208000027866 inflammatory disease Diseases 0.000 claims 1
- 125000000959 isobutyl group Chemical group [H]C([H])([H])C([H])(C([H])([H])[H])C([H])([H])* 0.000 claims 1
- 125000001449 isopropyl group Chemical group [H]C([H])([H])C([H])(*)C([H])([H])[H] 0.000 claims 1
- ZLTPDFXIESTBQG-UHFFFAOYSA-N isothiazole Chemical compound C=1C=NSC=1 ZLTPDFXIESTBQG-UHFFFAOYSA-N 0.000 claims 1
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 1
- 125000004108 n-butyl group Chemical group [H]C([H])([H])C([H])([H])C([H])([H])C([H])([H])* 0.000 claims 1
- 125000004123 n-propyl group Chemical group [H]C([H])([H])C([H])([H])C([H])([H])* 0.000 claims 1
- AHHWIHXENZJRFG-UHFFFAOYSA-N oxetane Chemical compound C1COC1 AHHWIHXENZJRFG-UHFFFAOYSA-N 0.000 claims 1
- UUEVFMOUBSLVJW-UHFFFAOYSA-N oxo-[[1-[2-[2-[2-[4-(oxoazaniumylmethylidene)pyridin-1-yl]ethoxy]ethoxy]ethyl]pyridin-4-ylidene]methyl]azanium;dibromide Chemical compound [Br-].[Br-].C1=CC(=C[NH+]=O)C=CN1CCOCCOCCN1C=CC(=C[NH+]=O)C=C1 UUEVFMOUBSLVJW-UHFFFAOYSA-N 0.000 claims 1
- 239000000546 pharmaceutical excipient Substances 0.000 claims 1
- 125000000999 tert-butyl group Chemical group [H]C([H])([H])C(*)(C([H])([H])[H])C([H])([H])[H] 0.000 claims 1
- 150000003536 tetrazoles Chemical class 0.000 claims 1
- VLLMWSRANPNYQX-UHFFFAOYSA-N thiadiazole Chemical compound C1=CSN=N1.C1=CSN=N1 VLLMWSRANPNYQX-UHFFFAOYSA-N 0.000 claims 1
- 150000003573 thiols Chemical group 0.000 claims 1
- 229930192474 thiophene Natural products 0.000 claims 1
- 150000003852 triazoles Chemical class 0.000 claims 1
- 0 CC=CC(NCC=CC(N(CC1)CC1N(C1=NC=CIC(N)=C11)N=C1c1ccc(*c2ccccc2)cc1)=O)=NC=C Chemical compound CC=CC(NCC=CC(N(CC1)CC1N(C1=NC=CIC(N)=C11)N=C1c1ccc(*c2ccccc2)cc1)=O)=NC=C 0.000 description 4
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201161507482P | 2011-07-13 | 2011-07-13 | |
| US61/507,482 | 2011-07-13 | ||
| PCT/US2012/046779 WO2013010136A2 (en) | 2011-07-13 | 2012-07-13 | Inhibitors of bruton's tyrosine kinase |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2014520863A JP2014520863A (ja) | 2014-08-25 |
| JP2014520863A5 true JP2014520863A5 (enExample) | 2015-09-03 |
Family
ID=47506961
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2014520391A Pending JP2014520863A (ja) | 2011-07-13 | 2012-07-13 | Ｂｒｕｔｏｎ型チロシンキナーゼの阻害剤 |
Country Status (13)
| Country | Link |
|---|---|
| US (2) | US9138436B2 (enExample) |
| EP (1) | EP2731612A4 (enExample) |
| JP (1) | JP2014520863A (enExample) |
| KR (1) | KR20140048968A (enExample) |
| CN (1) | CN103857396A (enExample) |
| AU (1) | AU2012283775A1 (enExample) |
| BR (1) | BR112014000653A2 (enExample) |
| CA (1) | CA2841080A1 (enExample) |
| EA (1) | EA201490265A1 (enExample) |
| MX (1) | MX2014000518A (enExample) |
| PH (1) | PH12014500122A1 (enExample) |
| WO (1) | WO2013010136A2 (enExample) |
| ZA (1) | ZA201400012B (enExample) |
Families Citing this family (80)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US20220213106A1 (en) * | 2006-09-22 | 2022-07-07 | Pharmacyclics Llc | Inhibitors of Bruton's Tyrosine Kinase |
| SG191724A1 (en) | 2011-01-11 | 2013-08-30 | Glaxosmithkline Llc | Combination |
| WO2012158795A1 (en) | 2011-05-17 | 2012-11-22 | Principia Biopharma Inc. | Pyrazolopyrimidine derivatives as tyrosine kinase inhibitors |
| HUE033019T2 (en) | 2011-05-17 | 2017-11-28 | Principia Biopharma Inc | Tyrosine kinase inhibitors |
| US9309250B2 (en) | 2011-06-22 | 2016-04-12 | Vertex Pharmaceuticals Incorporated | Substituted pyrrolo[2,3-b]pyrazines as ATR kinase inhibitors |
| KR20140048968A (ko) | 2011-07-13 | 2014-04-24 | 파마시클릭스, 인코포레이티드 | 브루톤형 티로신 키나제의 억제제 |
| HRP20190135T1 (hr) | 2011-07-19 | 2019-03-22 | Merck Sharp & Dohme B.V. | 4-imidazopiridazin-1-yl-benzamidi i 4-imidazotriazin-1-yl-benzamidi kao inhibitori btk |
| EP2548877A1 (en) | 2011-07-19 | 2013-01-23 | MSD Oss B.V. | 4-(5-Membered fused pyridinyl)benzamides as BTK-inhibitors |
| US9416132B2 (en) | 2011-07-21 | 2016-08-16 | Tolero Pharmaceuticals, Inc. | Substituted imidazo[1,2-b]pyridazines as protein kinase inhibitors |
| US8377946B1 (en) | 2011-12-30 | 2013-02-19 | Pharmacyclics, Inc. | Pyrazolo[3,4-d]pyrimidine and pyrrolo[2,3-d]pyrimidine compounds as kinase inhibitors |
| SI2892900T1 (en) | 2012-09-10 | 2018-01-31 | Principia Biopharma Inc. | Pyrazolopyrimidine compounds as kinase inhibitors |
| FI4190786T3 (fi) | 2012-12-07 | 2025-05-23 | Vertex Pharma | Atr-kinaasin estäjinä käyttökelpoisia yhdisteitä |
| EP2964249A1 (en) * | 2013-03-06 | 2016-01-13 | Acorda Therapeutics, Inc. | Therapeutic dosing of a neuregulin or a fragment thereof for treatment or prophylaxis of heart failure |
| US9152578B1 (en) * | 2013-03-12 | 2015-10-06 | Emc Corporation | Securing data replication, backup and mobility in cloud storage |
| RU2019119893A (ru) | 2013-03-14 | 2019-08-09 | Толеро Фармасьютикалз, Инк. | Ингибиторы jak2 и alk2 и способы их использования |
| EP2970286A1 (en) | 2013-03-15 | 2016-01-20 | Vertex Pharmaceuticals Inc. | Fused pyrazolopyrimidine derivatives useful as inhibitors of atr kinase |
| WO2014143242A1 (en) | 2013-03-15 | 2014-09-18 | Vertex Pharmaceuticals Incorporated | Compounds useful as inhibitors of atr kinase |
| EP2970289A1 (en) | 2013-03-15 | 2016-01-20 | Vertex Pharmaceuticals Inc. | Compounds useful as inhibitors of atr kinase |
| SI2970291T1 (sl) * | 2013-03-15 | 2022-07-29 | Janssen Pharmaceutica, N.V. | Postopki in vmesne spojine za pripravo zdravila |
| US8957080B2 (en) | 2013-04-09 | 2015-02-17 | Principia Biopharma Inc. | Tyrosine kinase inhibitors |
| GB201309085D0 (en) | 2013-05-20 | 2013-07-03 | Redx Pharma Ltd | Compounds |
| EP2999702A4 (en) * | 2013-05-21 | 2017-01-11 | Jiangsu Medolution Ltd. | Substituted pyrazolopyrimidines as kinases inhibitors |
| AU2014307437B2 (en) * | 2013-08-12 | 2016-12-15 | Taiho Pharmaceutical Co., Ltd. | Novel fused pyrimidine compound or salt thereof |
| AU2014324532A1 (en) | 2013-09-30 | 2016-04-21 | Pharmacyclics Llc | Inhibitors of Bruton's tyrosine kinase |
| CN103626774B (zh) * | 2013-11-20 | 2015-11-04 | 苏州明锐医药科技有限公司 | 伊鲁替尼的制备方法 |
| BR112016012794A2 (pt) | 2013-12-05 | 2017-08-08 | Acerta Pharma Bv | Combinação terapêutica de um inibidor de pi3k e um inibidor de btk |
| EP3077397B1 (en) | 2013-12-06 | 2019-09-18 | Vertex Pharmaceuticals Inc. | 2-amino-6-fluoro-n-[5-fluoro-pyridin-3-yl]pyrazolo[1,5-a]pyrimidin-3-carboxamide compound useful as atr kinase inhibitor, its preparation, different solid forms and radiolabelled derivatives thereof |
| US10272083B2 (en) | 2014-01-21 | 2019-04-30 | Acerta Pharma B.V. | Methods of treating chronic lymphocytic leukemia and small lymphocytic leukemia using a BTK inhibitor |
| 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. |
| US20170020878A1 (en) * | 2014-03-12 | 2017-01-26 | Novartis Ag | Combination comprising a btk inhibitor and an akt inhibitor |
| WO2015181633A2 (en) | 2014-04-11 | 2015-12-03 | Acerta Pharma B.V. | Methods of blocking the cxcr-4/sdf-1 signaling pathway with inhibitors of bruton's tyrosine kinase |
| 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 |
| CN103965201A (zh) * | 2014-04-30 | 2014-08-06 | 淮海工学院 | 一种合成依鲁替尼中间体4-氨基-3-(4-苯氧基苯基)-1H-吡唑并[3,4-d]嘧啶的方法 |
| HRP20200186T1 (hr) | 2014-06-05 | 2020-05-29 | Vertex Pharmaceuticals Inc. | Radioaktivno obilježeni derivati 2-amino-6-fluoro-n-[5-fluoro-piridin-3-il]-pirazolo[1,5-a]pirimidin-3-karboksamid spojeva koji se koriste kao inhibitori atr kinaze, priprava navedenih spojeva i njihovi različiti čvrsti oblici |
| GB201410430D0 (en) * | 2014-06-11 | 2014-07-23 | Redx Pharma Ltd | Compounds |
| JP6936007B2 (ja) | 2014-06-17 | 2021-09-15 | バーテックス ファーマシューティカルズ インコーポレイテッドＶｅｒｔｅｘ Ｐｈａｒｍａｃｅｕｔｉｃａｌｓ Ｉｎｃｏｒｐｏｒａｔｅｄ | Ｃｈｋ１阻害剤とａｔｒ阻害剤との組み合わせを使用してがんを処置する方法 |
| WO2015193740A2 (en) | 2014-06-17 | 2015-12-23 | Acerta Pharma B.V. | Therapeutic combinations of a btk inhibitor, a pi3k inhibitor and/or a jak-2 inhibitor |
| AT515941B1 (de) | 2014-07-29 | 2016-01-15 | Avl List Gmbh | Kondensationspartikelzähler mit einer Sättigungseinheit und einer nachgeschalteten Kondensationseinheit |
| CA2959602A1 (en) | 2014-08-01 | 2016-02-04 | Pharmacyclics Llc | Inhibitors of bruton's tyrosine kinase |
| HRP20211813T1 (hr) | 2014-08-11 | 2022-03-04 | Acerta Pharma B.V. | Terapeutske kombinacije inhibitora btk i inhibitora bcl-2 |
| TW201702218A (zh) | 2014-12-12 | 2017-01-16 | 美國杰克森實驗室 | 關於治療癌症、自體免疫疾病及神經退化性疾病之組合物及方法 |
| MA41197B1 (fr) | 2014-12-18 | 2021-01-29 | Principia Biopharma Inc | Traitement de le pemphigus |
| KR101858421B1 (ko) * | 2015-01-30 | 2018-05-15 | 다이호야쿠힌고교 가부시키가이샤 | 면역 질환의 예방 및/또는 치료제 |
| 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 |
| 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 |
| CN104844573A (zh) * | 2015-04-17 | 2015-08-19 | 中国药科大学 | 嘧啶类btk抑制剂、其制备方法及医药用途 |
| US20180305350A1 (en) | 2015-06-24 | 2018-10-25 | Principia Biopharma Inc. | Tyrosine kinase inhibitors |
| ES2797987T3 (es) | 2015-07-02 | 2020-12-04 | Acerta Pharma Bv | Formas sólidas y formulaciones de (S)-4-(8-amino-3-(1-(but-2-inoil)pirrolidin-2-il)imidazo[1,5-a]pirazin-1-il)-N-(piridin-2-il)benzamida |
| KR101766194B1 (ko) | 2015-08-07 | 2017-08-10 | 한국과학기술연구원 | RET 키나아제 저해제인 신규 3-(이속사졸-3-일)-피라졸로[3,4-d]피리미딘-4-아민 화합물 |
| KR102075886B1 (ko) * | 2015-09-01 | 2020-02-11 | 다이호야쿠힌고교 가부시키가이샤 | 신규한 피라졸로[3,4-d]피리미딘 화합물 또는 그 염 |
| EP4116303A1 (en) | 2015-09-16 | 2023-01-11 | Loxo Oncology, Inc. | Pyrazolopyrimidine derivatives as btk inhibitors for the treatment of cancer |
| EP3355926B1 (en) | 2015-09-30 | 2025-12-24 | Vertex Pharmaceuticals Inc. | Combination of dna damaging agents and atr inhibitors for use in a method for treating cancer using |
| MD3390395T2 (ro) | 2015-12-16 | 2021-02-28 | Loxo Oncology Inc | Compuși utili ca inhibitori ai kinazei |
| US10836745B2 (en) | 2015-12-24 | 2020-11-17 | Takeda Pharmaceutical Company Limited | Cocrystal, production method thereof, and medicament containing cocrystal |
| WO2017133630A1 (zh) * | 2016-02-05 | 2017-08-10 | 北京盛诺基医药科技有限公司 | 一种布鲁顿酪氨酸激酶抑制剂 |
| JP6972002B2 (ja) | 2016-03-11 | 2021-11-24 | エンジェル・ファーマシューティカル・カンパニー・リミテッド | ブルトン型チロシンキナーゼを調節する化合物及び方法 |
| EP3478273A1 (en) | 2016-06-29 | 2019-05-08 | 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 |
| WO2018033091A1 (zh) * | 2016-08-17 | 2018-02-22 | 深圳市塔吉瑞生物医药有限公司 | 用于抑制酪氨酸激酶活性的稠合双环类化合物 |
| CN108069974B (zh) * | 2016-11-15 | 2019-12-10 | 杭州和正医药有限公司 | 一种选择性布鲁顿酪氨酸激酶抑制剂及其应用 |
| TW201837040A (zh) * | 2017-03-15 | 2018-10-16 | 美商微拉製藥公司 | Cdpk1抑制劑及與其相關之組合物及方法 |
| CN107043366B (zh) * | 2017-04-25 | 2020-05-26 | 中国药科大学 | 4-氨基嘧啶类化合物、其制备方法及医药用途 |
| CN107383015B (zh) * | 2017-07-03 | 2019-11-08 | 四川大学华西医院 | 烷硫端基寡PEG修饰的氨基吡唑并[3,4-d]嘧啶衍生物及抗非小细胞肺癌的应用 |
| TW201920184A (zh) | 2017-08-17 | 2019-06-01 | 美國華盛頓大學 | Cdpk1抑制劑、組合物及與其相關之方法 |
| CN109422749B (zh) * | 2017-08-21 | 2023-01-24 | 重庆医药工业研究院有限责任公司 | 一种抑制单羧酸转运蛋白的嘧啶二酮衍生物 |
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| CA2959602A1 (en) | 2014-08-01 | 2016-02-04 | Pharmacyclics Llc | Inhibitors of bruton's tyrosine kinase |
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2012
- 2012-07-13 KR KR20147003521A patent/KR20140048968A/ko not_active Withdrawn
- 2012-07-13 BR BR112014000653A patent/BR112014000653A2/pt not_active IP Right Cessation
- 2012-07-13 PH PH1/2014/500122A patent/PH12014500122A1/en unknown
- 2012-07-13 EA EA201490265A patent/EA201490265A1/ru unknown
- 2012-07-13 CA CA2841080A patent/CA2841080A1/en not_active Abandoned
- 2012-07-13 CN CN201280044640.1A patent/CN103857396A/zh active Pending
- 2012-07-13 MX MX2014000518A patent/MX2014000518A/es unknown
- 2012-07-13 JP JP2014520391A patent/JP2014520863A/ja active Pending
- 2012-07-13 US US13/549,267 patent/US9138436B2/en active Active
- 2012-07-13 WO PCT/US2012/046779 patent/WO2013010136A2/en not_active Ceased
- 2012-07-13 EP EP20120811600 patent/EP2731612A4/en not_active Withdrawn
- 2012-07-13 AU AU2012283775A patent/AU2012283775A1/en not_active Abandoned
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2014
- 2014-01-06 ZA ZA2014/00012A patent/ZA201400012B/en unknown
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2015
- 2015-07-28 US US14/811,541 patent/US9862722B2/en active Active