JP2014513729A5 - - Google Patents
Download PDFInfo
- Publication number
- JP2014513729A5 JP2014513729A5 JP2014511503A JP2014511503A JP2014513729A5 JP 2014513729 A5 JP2014513729 A5 JP 2014513729A5 JP 2014511503 A JP2014511503 A JP 2014511503A JP 2014511503 A JP2014511503 A JP 2014511503A JP 2014513729 A5 JP2014513729 A5 JP 2014513729A5
- Authority
- JP
- Japan
- Prior art keywords
- unsubstituted
- substituted
- saturated
- alkyl
- cycloalkyl
- 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
- 125000000217 alkyl group Chemical group 0.000 claims 29
- 150000001875 compounds Chemical class 0.000 claims 22
- 229910052739 hydrogen Inorganic materials 0.000 claims 14
- 239000001257 hydrogen Substances 0.000 claims 14
- 125000000753 cycloalkyl group Chemical group 0.000 claims 11
- 125000000592 heterocycloalkyl group Chemical group 0.000 claims 10
- 125000001072 heteroaryl group Chemical group 0.000 claims 9
- 125000004191 (C1-C6) alkoxy group Chemical group 0.000 claims 8
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 7
- 125000003118 aryl group Chemical group 0.000 claims 7
- 125000004737 (C1-C6) haloalkoxy group Chemical group 0.000 claims 6
- 125000004093 cyano group Chemical group *C#N 0.000 claims 6
- 125000005843 halogen group Chemical group 0.000 claims 6
- 125000004404 heteroalkyl group Chemical group 0.000 claims 6
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 6
- 125000000171 (C1-C6) haloalkyl group Chemical group 0.000 claims 4
- 125000005549 heteroarylene group Chemical group 0.000 claims 4
- 125000005842 heteroatom Chemical group 0.000 claims 4
- 125000006588 heterocycloalkylene group Chemical group 0.000 claims 4
- 150000002431 hydrogen Chemical class 0.000 claims 4
- 229920006395 saturated elastomer Polymers 0.000 claims 4
- 125000002947 alkylene group Chemical group 0.000 claims 3
- 125000000732 arylene group Chemical group 0.000 claims 3
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 claims 3
- 125000002993 cycloalkylene group Chemical group 0.000 claims 3
- 229910052736 halogen Inorganic materials 0.000 claims 3
- 150000002367 halogens Chemical group 0.000 claims 3
- 125000004474 heteroalkylene group Chemical group 0.000 claims 3
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims 3
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 3
- 229910052760 oxygen Inorganic materials 0.000 claims 3
- 239000008194 pharmaceutical composition Substances 0.000 claims 3
- 229910052717 sulfur Inorganic materials 0.000 claims 3
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 claims 2
- -1 Methylamino, dimethylamino, 2-methylaminoethyl Chemical group 0.000 claims 2
- 125000001153 fluoro group Chemical group F* 0.000 claims 2
- 125000000325 methylidene group Chemical group [H]C([H])=* 0.000 claims 2
- 125000002950 monocyclic group Chemical group 0.000 claims 2
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 2
- 150000003839 salts Chemical class 0.000 claims 2
- 125000001424 substituent group Chemical group 0.000 claims 2
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 claims 1
- 125000004214 1-pyrrolidinyl group Chemical group [H]C1([H])N(*)C([H])([H])C([H])([H])C1([H])[H] 0.000 claims 1
- 208000023275 Autoimmune disease Diseases 0.000 claims 1
- GAWIXWVDTYZWAW-UHFFFAOYSA-N C[CH]O Chemical group C[CH]O GAWIXWVDTYZWAW-UHFFFAOYSA-N 0.000 claims 1
- 206010028980 Neoplasm Diseases 0.000 claims 1
- 125000004566 azetidin-1-yl group Chemical group N1(CCC1)* 0.000 claims 1
- 125000002393 azetidinyl group Chemical group 0.000 claims 1
- 125000002619 bicyclic group Chemical group 0.000 claims 1
- 201000011510 cancer Diseases 0.000 claims 1
- 229910052799 carbon Inorganic materials 0.000 claims 1
- 125000004432 carbon atom Chemical group C* 0.000 claims 1
- 125000004029 hydroxymethyl group Chemical group [H]OC([H])([H])* 0.000 claims 1
- 208000027866 inflammatory disease Diseases 0.000 claims 1
- 239000000546 pharmaceutical excipient Substances 0.000 claims 1
- 125000004194 piperazin-1-yl group Chemical group [H]N1C([H])([H])C([H])([H])N(*)C([H])([H])C1([H])[H] 0.000 claims 1
- 125000004193 piperazinyl group Chemical group 0.000 claims 1
- 125000000587 piperidin-1-yl group Chemical group [H]C1([H])N(*)C([H])([H])C([H])([H])C([H])([H])C1([H])[H] 0.000 claims 1
- 125000003386 piperidinyl group Chemical group 0.000 claims 1
- 125000000719 pyrrolidinyl group Chemical group 0.000 claims 1
- 125000003107 substituted aryl group Chemical group 0.000 claims 1
- 238000006467 substitution reaction Methods 0.000 claims 1
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 claims 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201161487233P | 2011-05-17 | 2011-05-17 | |
| US61/487,233 | 2011-05-17 | ||
| PCT/US2012/038214 WO2012158843A2 (en) | 2011-05-17 | 2012-05-16 | Kinase inhibitors |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2014513729A JP2014513729A (ja) | 2014-06-05 |
| JP2014513729A5 true JP2014513729A5 (enExample) | 2015-07-02 |
| JP6068451B2 JP6068451B2 (ja) | 2017-01-25 |
Family
ID=47177614
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2014511503A Active JP6068451B2 (ja) | 2011-05-17 | 2012-05-16 | キナーゼ阻害剤 |
Country Status (14)
| Country | Link |
|---|---|
| US (1) | US9580427B2 (enExample) |
| EP (1) | EP2710007B1 (enExample) |
| JP (1) | JP6068451B2 (enExample) |
| KR (1) | KR102052670B1 (enExample) |
| CN (1) | CN103717602B (enExample) |
| AU (1) | AU2012255759C1 (enExample) |
| BR (1) | BR112013029508B1 (enExample) |
| CA (1) | CA2836449C (enExample) |
| DK (1) | DK2710007T3 (enExample) |
| ES (1) | ES2770550T3 (enExample) |
| HU (1) | HUE048834T2 (enExample) |
| MX (1) | MX355728B (enExample) |
| PL (1) | PL2710007T3 (enExample) |
| WO (1) | WO2012158843A2 (enExample) |
Families Citing this family (94)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP2361248B1 (en) | 2008-06-27 | 2018-09-19 | Celgene CAR LLC | Heteroaryl compounds and uses thereof |
| US11351168B1 (en) | 2008-06-27 | 2022-06-07 | Celgene Car Llc | 2,4-disubstituted pyrimidines useful as kinase inhibitors |
| US8338439B2 (en) | 2008-06-27 | 2012-12-25 | Celgene Avilomics Research, Inc. | 2,4-disubstituted pyrimidines useful as kinase inhibitors |
| EP2603081B1 (en) | 2010-08-10 | 2016-10-05 | Celgene Avilomics Research, Inc. | Besylate salt of a btk inhibitor |
| US9238629B2 (en) | 2010-11-01 | 2016-01-19 | Celgene Avilomics Research, Inc. | Heteroaryl compounds and uses thereof |
| TWI545115B (zh) | 2010-11-01 | 2016-08-11 | 阿維拉製藥公司 | 雜環化合物及其用途 |
| WO2012064706A1 (en) | 2010-11-10 | 2012-05-18 | Avila Therapeutics, Inc. | Mutant-selective egfr inhibitors and uses thereof |
| 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 |
| JP2014520863A (ja) | 2011-07-13 | 2014-08-25 | ファーマサイクリックス，インク． | Ｂｒｕｔｏｎ型チロシンキナーゼの阻害剤 |
| EP2548877A1 (en) | 2011-07-19 | 2013-01-23 | MSD Oss B.V. | 4-(5-Membered fused pyridinyl)benzamides as BTK-inhibitors |
| BR112014001255B1 (pt) | 2011-07-19 | 2019-07-02 | Merck Sharp & Dohme B.V. | Composto, uso de um composto, combinação, composição farmacêutica, e, sal farmaceuticamente aceitável de um composto |
| AR088570A1 (es) | 2011-10-28 | 2014-06-18 | Celgene Avilomics Res Inc | Metodos para tratar una enfermedad o trastorno relacionado con la tirosina quinasa de bruton |
| 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 |
| PT2825042T (pt) | 2012-03-15 | 2018-11-16 | Celgene Car Llc | Sais de um inibidor de cinases do recetor do fator de crescimento epidérmico |
| CN104302178B (zh) | 2012-03-15 | 2018-07-13 | 西建卡尔有限责任公司 | 表皮生长因子受体激酶抑制剂的固体形式 |
| CA2868302A1 (en) | 2012-03-23 | 2013-09-26 | Dennis M. Brown | Compositions and methods to improve the therapeutic benefit of indirubin and analogs thereof, including meisoindigo |
| WO2013191965A1 (en) * | 2012-06-18 | 2013-12-27 | Principia Biopharma Inc. | Reversible covalent pyrrolo- or pyrazolopyrimidines useful for the treatment cancer and autoimmune diseases |
| NZ703495A (en) * | 2012-07-11 | 2018-02-23 | Blueprint Medicines Corp | Inhibitors of the fibroblast growth factor receptor |
| US9573958B2 (en) | 2012-08-31 | 2017-02-21 | Principia Biopharma, Inc. | Benzimidazole derivatives as ITK inhibitors |
| ES2644964T3 (es) | 2012-09-10 | 2017-12-01 | Principia Biopharma Inc. | Compuestos pirazolopirimidínicos comos inhibidores de cinasas |
| WO2014093230A2 (en) | 2012-12-10 | 2014-06-19 | Merck Patent Gmbh | Compositions and methods for the production of pyrimidine and pyridine compounds with btk inhibitory activity |
| WO2014100748A1 (en) | 2012-12-21 | 2014-06-26 | Celgene Avilomics Research, Inc. | Heteroaryl compounds and uses thereof |
| TWI629266B (zh) * | 2012-12-28 | 2018-07-11 | 藍印藥品公司 | 纖維母細胞生長因子受體之抑制劑 |
| KR20150119012A (ko) | 2013-02-08 | 2015-10-23 | 셀진 아빌로믹스 리서치, 인코포레이티드 | Erk 억제제 및 이의 용도 |
| US9346801B2 (en) | 2013-03-01 | 2016-05-24 | Amgen Inc. | Substituted 7-oxo-pyrido[2,3-d]pyrimidines and methods of use |
| TWI647220B (zh) | 2013-03-15 | 2019-01-11 | 美商西建卡爾有限責任公司 | 雜芳基化合物及其用途 |
| CA2907243C (en) | 2013-03-15 | 2021-12-28 | Celgene Avilomics Research, Inc. | Substituted dihydropyrimidopyrimidinone compounds and pharmaceutical compositions thereof use fgfr4 inhibitor |
| US9663524B2 (en) | 2013-03-15 | 2017-05-30 | Celgene Car Llc | Substituted pyrido[2,3-d]pyrimidines as protein kinase inhibitors |
| 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 |
| ES2761572T3 (es) * | 2013-07-11 | 2020-05-20 | Acea Therapeutics Inc | Derivados de pirimidina como inhibidores de quinasa |
| US9492471B2 (en) | 2013-08-27 | 2016-11-15 | Celgene Avilomics Research, Inc. | Methods of treating a disease or disorder associated with Bruton'S Tyrosine Kinase |
| CR20160203A (es) | 2013-09-30 | 2016-08-31 | Pharmacyclics Llc | Inhibidores de tirosina cinasa de bruton |
| HUE059037T2 (hu) | 2013-10-25 | 2022-10-28 | Blueprint Medicines Corp | Fibroblaszt növekedési faktor receptor gátlók |
| US9512084B2 (en) | 2013-11-29 | 2016-12-06 | Novartis Ag | Amino pyrimidine derivatives |
| EA201691169A1 (ru) | 2013-12-05 | 2016-09-30 | Асерта Фарма Б.В. | Терапевтическая комбинация ингибитора pi3k и ингибитора btk |
| JP6275846B2 (ja) * | 2013-12-05 | 2018-02-07 | エフ・ホフマン−ラ・ロシュ・アクチェンゲゼルシャフト | 求電子性官能基を有するヘテロアリールピリドン及びアザ−ピリドン化合物 |
| US9415049B2 (en) | 2013-12-20 | 2016-08-16 | Celgene Avilomics Research, Inc. | Heteroaryl compounds and uses thereof |
| WO2015108992A1 (en) | 2014-01-15 | 2015-07-23 | Blueprint Medicines Corporation | Heterobicyclic compounds and their use as fgfr4 receptor inhibitors |
| 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 |
| CA2937746C (en) | 2014-02-07 | 2020-09-01 | Principia Biopharma, Inc. | Quinolone derivatives as fibroblast growth factor receptor inhibitors |
| PT3107544T (pt) | 2014-02-21 | 2021-01-05 | Principia Biopharma Inc | Sais e forma sólida de um inibidor de btk |
| WO2015185998A2 (en) | 2014-04-11 | 2015-12-10 | Acerta Pharma B.V. | Methods of blocking the cxcr-4/sdf-1 signaling pathway with inhibitors of bone marrow x kinase |
| 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 |
| GB201410430D0 (en) | 2014-06-11 | 2014-07-23 | Redx Pharma Ltd | Compounds |
| TW201613644A (en) | 2014-06-17 | 2016-04-16 | Acerta Pharma Bv | Therapeutic combinations of a BTK inhibitor, a PI3K inhibitor, and/or a JAK-2 inhibitor |
| CN104945404B (zh) * | 2014-06-25 | 2018-09-14 | 广东东阳光药业有限公司 | 一种n-丙烯羰基哌啶衍生物的制备方法 |
| WO2016019233A1 (en) | 2014-08-01 | 2016-02-04 | Pharmacyclics Llc | Inhibitors of bruton's tyrosine kinase |
| TW201618783A (zh) | 2014-08-07 | 2016-06-01 | 艾森塔製藥公司 | 以布魯頓(Bruton)氏酪胺酸激酶(BTK)佔據和BTK再合成速率為基礎之治療癌症、免疫和自體免疫疾病及發炎性疾病之方法 |
| TW201618774A (zh) | 2014-08-11 | 2016-06-01 | 艾森塔製藥公司 | 使用ｂｔｋ抑制劑透過調變腫瘤微環境來治療實體腫瘤及其他疾病之方法 |
| SMT202200285T1 (it) | 2014-08-11 | 2022-09-14 | Acerta Pharma Bv | Combinazioni terapeutiche di un inibitore di btk, un inibitore di pd-1 e/o un inibitore di pd-l1 |
| ES2900184T3 (es) | 2014-08-11 | 2022-03-16 | Acerta Pharma Bv | Combinaciones terapéuticas de un inhibidor de BTK y un inhibidor de BCL-2 |
| AR101504A1 (es) | 2014-08-11 | 2016-12-21 | Acerta Pharma Bv | Combinaciones terapéuticas de un inhibidor de la btk, un inhibidor de la pi3k, un inhibidor de la jak-2, y/o un inhibidor de la cdk4/6 |
| TW201613892A (en) | 2014-08-13 | 2016-04-16 | Celgene Avilomics Res Inc | Forms and compositions of an ERK inhibitor |
| CN105524068B (zh) | 2014-09-30 | 2017-11-24 | 上海海雁医药科技有限公司 | 氮杂双环衍生物、其制法与医药上的用途 |
| WO2016060963A1 (en) * | 2014-10-14 | 2016-04-21 | Sunshine Lake Pharma Co., Ltd. | Substituted heteroaryl compounds and methods of use |
| CN105601573B (zh) | 2014-11-24 | 2021-07-02 | 中国科学院上海药物研究所 | 2-氨基嘧啶类化合物及其药物组合物和应用 |
| WO2016087994A1 (en) | 2014-12-05 | 2016-06-09 | Acerta Pharma B.V. | Btk inhibitors to treat solid tumors through modulation of the tumor microenvironment |
| US10485797B2 (en) | 2014-12-18 | 2019-11-26 | Principia Biopharma Inc. | Treatment of pemphigus |
| CN105481862B (zh) * | 2015-01-21 | 2018-08-21 | 中国科学院合肥物质科学研究院 | Flt3激酶的新型抑制剂及其用途 |
| US10266535B2 (en) | 2015-01-21 | 2019-04-23 | Hefei Institutes Of Physical Science, Chinese Academy Of Sciences | Inhibitor of FLT3 kinase and use thereof |
| CN104774184A (zh) * | 2015-04-17 | 2015-07-15 | 中国药科大学 | α-氰基-α,β-不饱和酰胺类化合物及其医药用途 |
| WO2016191172A1 (en) * | 2015-05-22 | 2016-12-01 | Principia Biopharma Inc. | Quinolone derivatives as fibroblast growth factor receptor inhibitors |
| DK3303334T3 (da) * | 2015-06-03 | 2021-06-28 | Principia Biopharma Inc | Tyrosinkinasehæmmere |
| MA42242A (fr) | 2015-06-24 | 2018-05-02 | Principia Biopharma Inc | Inhibiteurs de la tyrosine kinase |
| HUE049989T2 (hu) | 2015-07-02 | 2020-11-30 | Acerta Pharma Bv | (S)-4-(8-amino-3-(1-(but-2-inoil)pirrolidin-2-il)imidazo[1,5-a]pirazin-1-il)-N-(piridin-2-il)benzamid szilárd alakjai és készítményei |
| CN108137559B (zh) * | 2015-07-09 | 2021-11-02 | 默克专利有限公司 | 用作btk抑制剂的嘧啶衍生物及其用途 |
| WO2017027567A1 (en) | 2015-08-11 | 2017-02-16 | Principia Biopharma, Inc. | Processes for preparing an fgfr inhibitor |
| WO2017033113A1 (en) | 2015-08-21 | 2017-03-02 | Acerta Pharma B.V. | Therapeutic combinations of a mek inhibitor and a btk inhibitor |
| MA44909A (fr) | 2015-09-15 | 2018-07-25 | Acerta Pharma Bv | Association thérapeutique d'un inhibiteur du cd19 et d'un inhibiteur de la btk |
| WO2017046746A1 (en) | 2015-09-15 | 2017-03-23 | Acerta Pharma B.V. | Therapeutic combinations of a btk inhibitor and a gitr binding molecule, a 4-1bb agonist, or an ox40 agonist |
| WO2017046604A1 (en) | 2015-09-16 | 2017-03-23 | Redx Pharma Plc | Pyrazolopyrimidine derivatives as btk inhibitors for the treatment of cancer |
| MA55064A (fr) | 2015-12-16 | 2021-09-29 | Loxo Oncology Inc | Composés utilisés comme inhibiteurs de kinase |
| HUE052893T2 (hu) | 2016-01-13 | 2021-05-28 | Acerta Pharma Bv | Antifolát és BTK-gátló terápiás kombinációi |
| WO2017134684A2 (en) * | 2016-02-01 | 2017-08-10 | Natco Pharma Limited | An improved process for the preparation of ibrutinib |
| IL261957B (en) | 2016-03-28 | 2022-07-01 | Incyte Corp | Pyrrolotriazine compounds as TAM inhibitors |
| CN107513068A (zh) * | 2016-06-16 | 2017-12-26 | 中国科学院上海药物研究所 | 一种具有fgfr抑制活性的新型化合物及其制备和应用 |
| 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 |
| CN109311883B (zh) * | 2017-02-09 | 2021-03-19 | 合肥合源药业有限公司 | Flt3激酶抑制剂或其盐的晶型及其制备方法 |
| CN108498477A (zh) * | 2017-02-27 | 2018-09-07 | 江苏奥赛康药业股份有限公司 | 一种2-氨基嘧啶类化合物的药用组合物及其制备方法 |
| CN109970740A (zh) * | 2017-12-27 | 2019-07-05 | 广东众生药业股份有限公司 | 4-氨基-嘧啶并氮杂环衍生物及其制备方法和用途 |
| WO2020043321A1 (en) | 2018-08-31 | 2020-03-05 | Stichting Katholieke Universiteit | Synergistic combinations of amino acid depletion agent sensitizers (aadas) and amino acid depletion agents (aada), and therapeutic methods of use thereof |
| PH12022550494A1 (en) * | 2019-09-19 | 2023-02-27 | Totus Medicines Inc | Therapeutic conjugates |
| CA3154257A1 (en) | 2019-10-14 | 2021-04-22 | Principia Biopharma Inc. | Methods for treating immune thrombocytopenia 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 |
| WO2021142124A1 (en) | 2020-01-08 | 2021-07-15 | Principia Biopharma Inc. | Topical pharmaceutical compositions comprising 2-[3-[4-amino-3-(2-fluoro-4-phenoxy-phenyl)-1h-pyrazolo[3,4-d]pyrimidin-1-yl]piperidine-1-carbonyl]-4,4-dimethylpent-2-enenitrile |
| 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 |
| JP2023538060A (ja) * | 2020-08-17 | 2023-09-06 | 貝達薬業股▲ふん▼有限公司 | 二環化合物、それを含む組成物、及びそれらの使用 |
| CN112358468B (zh) * | 2020-11-10 | 2022-03-22 | 德州德药制药有限公司 | 一种工业化合成azd9291的方法 |
| JP2024505328A (ja) * | 2020-12-18 | 2024-02-06 | アンフィスタ セラピューティクス リミテッド | 標的化されたタンパク質分解のための新規の二官能性分子 |
| CN115073467B (zh) * | 2021-03-15 | 2024-03-15 | 中国科学院上海药物研究所 | 一种嘧啶并咪唑类化合物及其药用组合物和应用 |
| WO2022198024A1 (en) * | 2021-03-18 | 2022-09-22 | Totus Medicines Inc. | Therapeutic conjugates |
| CN114605418B (zh) * | 2022-03-15 | 2023-09-05 | 广东医科大学附属医院 | 一类具有抗肿瘤活性的依鲁替尼丙烯酰胺类衍生物及其合成方法与应用 |
| CN119504835B (zh) * | 2024-11-21 | 2025-10-17 | 南开大学 | 一种以含硅基团为疏水标签的btk蛋白降解剂及其制备方法、药物组合物和应用 |
Family Cites Families (47)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| BE601150A (enExample) * | ||||
| JPS5617367A (en) | 1979-07-23 | 1981-02-19 | Fuji Xerox Co Ltd | Magnetic brush developing unit |
| JPS5663950A (en) | 1979-10-30 | 1981-05-30 | Mitsubishi Chem Ind Ltd | Cyclopropanecarboxylic ester |
| FR2535721A1 (fr) | 1982-11-08 | 1984-05-11 | Sanofi Sa | Derives de la piperidinedione protecteurs du myocarde presentant une acticite antiarythmique, leur procede de preparation et les medicaments qui contiennent lesdits derives |
| US4911920A (en) | 1986-07-30 | 1990-03-27 | Alcon Laboratories, Inc. | Sustained release, comfort formulation for glaucoma therapy |
| FR2588189B1 (fr) | 1985-10-03 | 1988-12-02 | Merck Sharp & Dohme | Composition pharmaceutique de type a transition de phase liquide-gel |
| DE3609982A1 (de) * | 1986-03-25 | 1987-10-01 | Bayer Ag | Cyclobutan-diester-dinitrile, verfahren zu ihrer herstellung und ihre verwendung |
| JP2518353B2 (ja) | 1988-06-09 | 1996-07-24 | 住友化学工業株式会社 | シアノ酢酸アミド誘導体およびその製造中間体 |
| FI96311C (fi) | 1989-12-04 | 1996-06-10 | Squibb Bristol Myers Co | Menetelmä farmaseuttisesti käyttökelpoisten 6-(1-hydroksietyyli)-3-(substituoitu tio)-7-okso-1-atsabisyklo/3.2.0/hept-2-eeni-2-karboksyylihappojohdannaisten valmistamiseksi |
| JPH04177244A (ja) | 1990-11-10 | 1992-06-24 | Konica Corp | ハロゲン化銀写真感光材料 |
| DK0495421T3 (da) | 1991-01-15 | 1996-12-09 | Alcon Lab Inc | Anvendelse af carragenaner i topiske ophthalmiske sammensætninger |
| US5212162A (en) | 1991-03-27 | 1993-05-18 | Alcon Laboratories, Inc. | Use of combinations gelling polysaccharides and finely divided drug carrier substrates in topical ophthalmic compositions |
| GB9406137D0 (en) * | 1994-03-28 | 1994-05-18 | Erba Carlo Spa | N-substituted beta-aryl- and betaheteroaryl-alpha-cyanoacrylamide derivatives and process for their preparation |
| US6309853B1 (en) | 1994-08-17 | 2001-10-30 | The Rockfeller University | Modulators of body weight, corresponding nucleic acids and proteins, and diagnostic and therapeutic uses thereof |
| US6331555B1 (en) * | 1995-06-01 | 2001-12-18 | University Of California | Treatment of platelet derived growth factor related disorders such as cancers |
| WO1996040629A1 (en) * | 1995-06-07 | 1996-12-19 | Sugen, Inc. | Tyrphostin-like compounds for the treatment of cell proliferative disorders or cell differentiation disorders |
| HUP0001603A3 (en) | 1997-03-14 | 2004-05-28 | Basf Ag | Cycloalkylalkanecarboxamides and the production and use thereof |
| IL125947A0 (en) | 1997-09-17 | 1999-04-11 | American Cyanamid Co | 3-(1,2-benzisothiazol- and isoxazol-5-yl)-2,4(1h,3h)-pyrimidinedione or thione and 3-(1,2-benzisothiazol- and isoxazol-5-yl)-4(3)-pyrimidinone or thione herbicidal agents |
| US6225346B1 (en) | 1997-10-24 | 2001-05-01 | Sugen, Inc. | Tyrphostin like compounds |
| MXPA03008560A (es) * | 2001-03-22 | 2004-06-30 | Abbot Gmbh & Co Kg | Pirazolopirimidinas como agentes terapeuticos. |
| JP3991812B2 (ja) | 2001-12-11 | 2007-10-17 | 住友化学株式会社 | エステル化合物およびその用途 |
| US7851411B2 (en) * | 2001-12-19 | 2010-12-14 | Basf Se | α-Cyanoacrylates |
| NI200300043A (es) | 2002-03-28 | 2003-11-05 | Warner Lambert Co | AMINOACIDOS CON AFINIDAD POR LA PROTEINA a2DELTA. |
| GB0219024D0 (en) | 2002-08-15 | 2002-09-25 | Pfizer Ltd | Synergistic combinations |
| CA2533763C (en) * | 2003-08-01 | 2012-11-20 | Chugai Seiyaku Kabushiki Kaisha | Cyanoamide compounds useful as malonyl-coa decarboxylase inhibitors |
| WO2005023773A1 (en) | 2003-09-04 | 2005-03-17 | Pfizer Limited | Process for the preparation of substituted aryl pyrazoles |
| GB0322140D0 (en) | 2003-09-22 | 2003-10-22 | Pfizer Ltd | Combinations |
| BRPI0414798A (pt) | 2003-09-25 | 2006-11-21 | Warner Lambert Co | métodos para usar aminoácidos com afinidade para a proteìna alfa2delta |
| JP4552456B2 (ja) | 2004-02-27 | 2010-09-29 | 住友化学株式会社 | エステル化合物およびその用途 |
| US20060079494A1 (en) * | 2004-09-27 | 2006-04-13 | Santi Daniel V | Specific kinase inhibitors |
| EP1647549A1 (en) * | 2004-10-14 | 2006-04-19 | Laboratoire Theramex | Indazoles, benzisoxazoles and benzisothiazoles as estrogenic agents |
| US20080176865A1 (en) | 2005-06-15 | 2008-07-24 | Pfizer Limited | Substituted arylpyrazoles |
| US20080146643A1 (en) | 2005-06-15 | 2008-06-19 | Pfizer Limited | Combination |
| US20070149464A1 (en) | 2005-06-15 | 2007-06-28 | Pfizer Inc. | Combination |
| US7645786B2 (en) | 2005-06-15 | 2010-01-12 | Pfizer Inc. | Substituted arylpyrazoles |
| EP1893581B1 (en) | 2005-06-15 | 2010-01-27 | Pfizer Limited | Substituted arylpyrazoles for use against parasitites |
| US20100292229A1 (en) * | 2006-06-30 | 2010-11-18 | The Board Of Regents Of The University Of Texas System | Tryphostin-analogs for the treatment of cell proliferative diseases |
| HUE028086T2 (en) * | 2006-09-22 | 2016-11-28 | Pharmacyclics Llc | Inhibitors of bruton's tyrosine kinase |
| KR20090086080A (ko) | 2006-11-23 | 2009-08-10 | 노파르티스 아게 | 피리미딘 및 그의 ｃｘｃｒ2 수용체 길항제로서의 용도 |
| US8450337B2 (en) * | 2008-09-30 | 2013-05-28 | Moleculin, Llc | Methods of treating skin disorders with caffeic acid analogs |
| US7718662B1 (en) * | 2009-10-12 | 2010-05-18 | Pharmacyclics, Inc. | Pyrazolo-pyrimidine inhibitors of bruton's tyrosine kinase |
| CN102711765A (zh) * | 2009-11-16 | 2012-10-03 | 加利福尼亚大学董事会 | 激酶抑制剂 |
| JP5655527B2 (ja) * | 2009-12-02 | 2015-01-21 | 住友化学株式会社 | （ｚ）−シアノアルケニルシクロプロパンカルボン酸化合物の製造方法 |
| CN101880243A (zh) | 2010-06-04 | 2010-11-10 | 贵阳柏丝特化工有限公司 | 一种含氟氰拟除虫菊酯化合物及其合成方法与用途 |
| US9187487B2 (en) * | 2011-05-17 | 2015-11-17 | Principia Biopharma, Inc. | Azaindole derivatives as tyrosine kinase inhibitors |
| WO2012158810A1 (en) * | 2011-05-17 | 2012-11-22 | Principia Biopharma Inc. | Tyrosine kinase inhibitors |
| HUE033019T2 (en) * | 2011-05-17 | 2017-11-28 | Principia Biopharma Inc | Tyrosine kinase inhibitors |
-
2012
- 2012-05-16 JP JP2014511503A patent/JP6068451B2/ja active Active
- 2012-05-16 US US14/118,541 patent/US9580427B2/en active Active
- 2012-05-16 HU HUE12785097A patent/HUE048834T2/hu unknown
- 2012-05-16 WO PCT/US2012/038214 patent/WO2012158843A2/en not_active Ceased
- 2012-05-16 ES ES12785097T patent/ES2770550T3/es active Active
- 2012-05-16 MX MX2013013415A patent/MX355728B/es active IP Right Grant
- 2012-05-16 CA CA2836449A patent/CA2836449C/en active Active
- 2012-05-16 DK DK12785097.2T patent/DK2710007T3/da active
- 2012-05-16 BR BR112013029508-2A patent/BR112013029508B1/pt active IP Right Grant
- 2012-05-16 CN CN201280024118.7A patent/CN103717602B/zh active Active
- 2012-05-16 KR KR1020137031023A patent/KR102052670B1/ko active Active
- 2012-05-16 EP EP12785097.2A patent/EP2710007B1/en active Active
- 2012-05-16 AU AU2012255759A patent/AU2012255759C1/en active Active
- 2012-05-16 PL PL12785097T patent/PL2710007T3/pl unknown