JP2017531000A5 - - Google Patents
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- Publication number
- JP2017531000A5 JP2017531000A5 JP2017519817A JP2017519817A JP2017531000A5 JP 2017531000 A5 JP2017531000 A5 JP 2017531000A5 JP 2017519817 A JP2017519817 A JP 2017519817A JP 2017519817 A JP2017519817 A JP 2017519817A JP 2017531000 A5 JP2017531000 A5 JP 2017531000A5
- Authority
- JP
- Japan
- Prior art keywords
- cycloalkyl
- alkyl
- membered heterocyclyl
- independently
- membered heteroaryl
- 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
- 125000000623 heterocyclic group Chemical group 0.000 claims 30
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 claims 17
- 150000001875 compounds Chemical class 0.000 claims 17
- 125000006570 (C5-C6) heteroaryl group Chemical group 0.000 claims 15
- -1 C 1 -C 6 alkoxyl Chemical group 0.000 claims 15
- 125000000217 alkyl group Chemical group 0.000 claims 14
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 14
- 125000001072 heteroaryl group Chemical group 0.000 claims 10
- 125000000882 C2-C6 alkenyl group Chemical group 0.000 claims 9
- 125000003601 C2-C6 alkynyl group Chemical group 0.000 claims 9
- 229910052799 carbon Inorganic materials 0.000 claims 9
- 125000000753 cycloalkyl group Chemical group 0.000 claims 9
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 8
- 125000004890 (C1-C6) alkylamino group Chemical group 0.000 claims 7
- 125000003118 aryl group Chemical group 0.000 claims 7
- 201000010099 disease Diseases 0.000 claims 7
- 125000006710 (C2-C12) alkenyl group Chemical group 0.000 claims 6
- 125000006711 (C2-C12) alkynyl group Chemical group 0.000 claims 6
- 125000006577 C1-C6 hydroxyalkyl group Chemical group 0.000 claims 5
- 125000003282 alkyl amino group Chemical group 0.000 claims 5
- 125000001559 cyclopropyl group Chemical group [H]C1([H])C([H])([H])C1([H])* 0.000 claims 5
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims 5
- 125000001449 isopropyl group Chemical group [H]C([H])([H])C([H])(*)C([H])([H])[H] 0.000 claims 5
- 230000001404 mediated effect Effects 0.000 claims 5
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 5
- 125000004123 n-propyl group Chemical group [H]C([H])([H])C([H])([H])C([H])([H])* 0.000 claims 5
- 229910052757 nitrogen Inorganic materials 0.000 claims 5
- 239000008194 pharmaceutical composition Substances 0.000 claims 5
- 125000004642 (C1-C12) alkoxy group Chemical group 0.000 claims 4
- 102000001253 Protein Kinase Human genes 0.000 claims 4
- 206010052779 Transplant rejections Diseases 0.000 claims 4
- 125000003545 alkoxy group Chemical group 0.000 claims 4
- 125000002947 alkylene group Chemical group 0.000 claims 4
- 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 4
- 108060006633 protein kinase Proteins 0.000 claims 4
- 125000000171 (C1-C6) haloalkyl group Chemical group 0.000 claims 3
- 125000004103 aminoalkyl group Chemical group 0.000 claims 3
- 239000003814 drug Substances 0.000 claims 3
- 229940124597 therapeutic agent Drugs 0.000 claims 3
- 125000006656 (C2-C4) alkenyl group Chemical group 0.000 claims 2
- 125000006650 (C2-C4) alkynyl group Chemical group 0.000 claims 2
- 125000004066 1-hydroxyethyl group Chemical group [H]OC([H])([*])C([H])([H])[H] 0.000 claims 2
- 125000000954 2-hydroxyethyl group Chemical group [H]C([*])([H])C([H])([H])O[H] 0.000 claims 2
- MSYGAHOHLUJIKV-UHFFFAOYSA-N 3,5-dimethyl-1-(3-nitrophenyl)-1h-pyrazole-4-carboxylic acid ethyl ester Chemical compound CC1=C(C(=O)OCC)C(C)=NN1C1=CC=CC([N+]([O-])=O)=C1 MSYGAHOHLUJIKV-UHFFFAOYSA-N 0.000 claims 2
- QOXOZONBQWIKDA-UHFFFAOYSA-N 3-hydroxypropyl Chemical group [CH2]CCO QOXOZONBQWIKDA-UHFFFAOYSA-N 0.000 claims 2
- 102000042838 JAK family Human genes 0.000 claims 2
- 150000001204 N-oxides Chemical class 0.000 claims 2
- 102000011017 Type 4 Cyclic Nucleotide Phosphodiesterases Human genes 0.000 claims 2
- 108010037584 Type 4 Cyclic Nucleotide Phosphodiesterases Proteins 0.000 claims 2
- 239000003795 chemical substances by application Substances 0.000 claims 2
- 125000002768 hydroxyalkyl group Chemical group 0.000 claims 2
- 125000002883 imidazolyl group Chemical group 0.000 claims 2
- 125000002950 monocyclic group Chemical group 0.000 claims 2
- 125000002757 morpholinyl group Chemical group 0.000 claims 2
- 125000004193 piperazinyl group Chemical group 0.000 claims 2
- 125000003226 pyrazolyl group Chemical group 0.000 claims 2
- 125000000714 pyrimidinyl group Chemical group 0.000 claims 2
- 125000000719 pyrrolidinyl group Chemical group 0.000 claims 2
- 150000003839 salts Chemical class 0.000 claims 2
- SNOOUWRIMMFWNE-UHFFFAOYSA-M sodium;6-[(3,4,5-trimethoxybenzoyl)amino]hexanoate Chemical compound [Na+].COC1=CC(C(=O)NCCCCCC([O-])=O)=CC(OC)=C1OC SNOOUWRIMMFWNE-UHFFFAOYSA-M 0.000 claims 2
- 239000012453 solvate Substances 0.000 claims 2
- 208000024893 Acute lymphoblastic leukemia Diseases 0.000 claims 1
- 208000031261 Acute myeloid leukaemia Diseases 0.000 claims 1
- 201000001320 Atherosclerosis Diseases 0.000 claims 1
- 208000023275 Autoimmune disease Diseases 0.000 claims 1
- 208000032791 BCR-ABL1 positive chronic myelogenous leukemia Diseases 0.000 claims 1
- 208000006545 Chronic Obstructive Pulmonary Disease Diseases 0.000 claims 1
- 208000011231 Crohn disease Diseases 0.000 claims 1
- 201000004624 Dermatitis Diseases 0.000 claims 1
- 208000032027 Essential Thrombocythemia Diseases 0.000 claims 1
- 208000004262 Food Hypersensitivity Diseases 0.000 claims 1
- 206010016946 Food allergy Diseases 0.000 claims 1
- 101000932478 Homo sapiens Receptor-type tyrosine-protein kinase FLT3 Proteins 0.000 claims 1
- 208000003456 Juvenile Arthritis Diseases 0.000 claims 1
- 206010059176 Juvenile idiopathic arthritis Diseases 0.000 claims 1
- 208000005777 Lupus Nephritis Diseases 0.000 claims 1
- 229940121948 Muscarinic receptor antagonist Drugs 0.000 claims 1
- 206010028980 Neoplasm Diseases 0.000 claims 1
- 201000004681 Psoriasis Diseases 0.000 claims 1
- 201000001263 Psoriatic Arthritis Diseases 0.000 claims 1
- 208000036824 Psoriatic arthropathy Diseases 0.000 claims 1
- 102100020718 Receptor-type tyrosine-protein kinase FLT3 Human genes 0.000 claims 1
- 208000021386 Sjogren Syndrome Diseases 0.000 claims 1
- 206010067584 Type 1 diabetes mellitus Diseases 0.000 claims 1
- 208000024780 Urticaria Diseases 0.000 claims 1
- 239000002671 adjuvant Substances 0.000 claims 1
- 239000000556 agonist Substances 0.000 claims 1
- 208000026935 allergic disease Diseases 0.000 claims 1
- 208000028004 allergic respiratory disease Diseases 0.000 claims 1
- 239000002260 anti-inflammatory agent Substances 0.000 claims 1
- 229940121363 anti-inflammatory agent Drugs 0.000 claims 1
- 230000001028 anti-proliverative effect Effects 0.000 claims 1
- 229940125715 antihistaminic agent Drugs 0.000 claims 1
- 239000000739 antihistaminic agent Substances 0.000 claims 1
- 239000002246 antineoplastic agent Substances 0.000 claims 1
- 125000000732 arylene group Chemical group 0.000 claims 1
- 208000006673 asthma Diseases 0.000 claims 1
- 125000004429 atom Chemical group 0.000 claims 1
- 208000010668 atopic eczema Diseases 0.000 claims 1
- 239000005441 aurora Substances 0.000 claims 1
- 201000011510 cancer Diseases 0.000 claims 1
- 125000004432 carbon atom Chemical group C* 0.000 claims 1
- 239000000969 carrier Substances 0.000 claims 1
- 210000004027 cell Anatomy 0.000 claims 1
- 239000000812 cholinergic antagonist Substances 0.000 claims 1
- 239000003246 corticosteroid Substances 0.000 claims 1
- 229960001334 corticosteroids Drugs 0.000 claims 1
- 125000001995 cyclobutyl group Chemical group [H]C1([H])C([H])([H])C([H])(*)C1([H])[H] 0.000 claims 1
- 229940127089 cytotoxic agent Drugs 0.000 claims 1
- 201000001981 dermatomyositis Diseases 0.000 claims 1
- 210000003743 erythrocyte Anatomy 0.000 claims 1
- 235000020932 food allergy Nutrition 0.000 claims 1
- 125000002541 furyl group Chemical group 0.000 claims 1
- 125000001188 haloalkyl group Chemical group 0.000 claims 1
- 150000002391 heterocyclic compounds Chemical class 0.000 claims 1
- 230000002519 immonomodulatory effect Effects 0.000 claims 1
- 229940125721 immunosuppressive agent Drugs 0.000 claims 1
- 239000003018 immunosuppressive agent Substances 0.000 claims 1
- 125000003453 indazolyl group Chemical group N1N=C(C2=C1C=CC=C2)* 0.000 claims 1
- 208000027866 inflammatory disease Diseases 0.000 claims 1
- 230000002757 inflammatory effect Effects 0.000 claims 1
- 239000003112 inhibitor Substances 0.000 claims 1
- 239000002919 insect venom Substances 0.000 claims 1
- 125000001786 isothiazolyl group Chemical group 0.000 claims 1
- 125000000842 isoxazolyl group Chemical group 0.000 claims 1
- 206010025135 lupus erythematosus Diseases 0.000 claims 1
- 239000002207 metabolite Substances 0.000 claims 1
- 125000000956 methoxy group Chemical group [H]C([H])([H])O* 0.000 claims 1
- 239000000203 mixture Substances 0.000 claims 1
- 206010028537 myelofibrosis Diseases 0.000 claims 1
- 125000004433 nitrogen atom Chemical group N* 0.000 claims 1
- 210000000056 organ Anatomy 0.000 claims 1
- 125000001715 oxadiazolyl group Chemical group 0.000 claims 1
- 125000002971 oxazolyl group Chemical group 0.000 claims 1
- 239000000546 pharmaceutical excipient Substances 0.000 claims 1
- 230000002265 prevention Effects 0.000 claims 1
- 239000000651 prodrug Substances 0.000 claims 1
- 229940002612 prodrug Drugs 0.000 claims 1
- 230000002062 proliferating effect Effects 0.000 claims 1
- 208000005069 pulmonary fibrosis Diseases 0.000 claims 1
- 125000003373 pyrazinyl group Chemical group 0.000 claims 1
- 125000002098 pyridazinyl group Chemical group 0.000 claims 1
- 125000005494 pyridonyl group Chemical group 0.000 claims 1
- 125000004076 pyridyl group Chemical group 0.000 claims 1
- 125000000168 pyrrolyl group Chemical group 0.000 claims 1
- 239000000018 receptor agonist Substances 0.000 claims 1
- 229940044601 receptor agonist Drugs 0.000 claims 1
- 230000001105 regulatory effect Effects 0.000 claims 1
- 206010039073 rheumatoid arthritis Diseases 0.000 claims 1
- 201000009890 sinusitis Diseases 0.000 claims 1
- 230000003637 steroidlike Effects 0.000 claims 1
- 125000001424 substituent group Chemical group 0.000 claims 1
- 208000011580 syndromic disease Diseases 0.000 claims 1
- 201000000596 systemic lupus erythematosus Diseases 0.000 claims 1
- 125000003831 tetrazolyl group Chemical group 0.000 claims 1
- 125000001113 thiadiazolyl group Chemical group 0.000 claims 1
- 125000000335 thiazolyl group Chemical group 0.000 claims 1
- 125000001544 thienyl group Chemical group 0.000 claims 1
- 125000004306 triazinyl group Chemical group 0.000 claims 1
- 125000001425 triazolyl group Chemical group 0.000 claims 1
- 231100000611 venom Toxicity 0.000 claims 1
- 208000034280 venom allergy Diseases 0.000 claims 1
- XLSZMDLNRCVEIJ-UHFFFAOYSA-N Cc1c[nH]cn1 Chemical compound Cc1c[nH]cn1 XLSZMDLNRCVEIJ-UHFFFAOYSA-N 0.000 description 2
- HMMPHXCOTBASBC-UHFFFAOYSA-N Cc1cc2n[nH]cc2cc1 Chemical compound Cc1cc2n[nH]cc2cc1 HMMPHXCOTBASBC-UHFFFAOYSA-N 0.000 description 2
- XKVUYEYANWFIJX-UHFFFAOYSA-N Cc1n[nH]cc1 Chemical compound Cc1n[nH]cc1 XKVUYEYANWFIJX-UHFFFAOYSA-N 0.000 description 2
- RIKMMFOAQPJVMX-UHFFFAOYSA-N Cc1c[nH]nc1 Chemical compound Cc1c[nH]nc1 RIKMMFOAQPJVMX-UHFFFAOYSA-N 0.000 description 1
- DCUNRLLJHAWKRZ-UHFFFAOYSA-N Cc1cc2c[nH]nc2cc1 Chemical compound Cc1cc2c[nH]nc2cc1 DCUNRLLJHAWKRZ-UHFFFAOYSA-N 0.000 description 1
- LXBGSDVWAMZHDD-UHFFFAOYSA-N Cc1ncc[nH]1 Chemical compound Cc1ncc[nH]1 LXBGSDVWAMZHDD-UHFFFAOYSA-N 0.000 description 1
- CGCHCLICSHIAAM-UHFFFAOYSA-N Ic1ccc2[nH]ncc2c1 Chemical compound Ic1ccc2[nH]ncc2c1 CGCHCLICSHIAAM-UHFFFAOYSA-N 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201462063460P | 2014-10-14 | 2014-10-14 | |
| US62/063,460 | 2014-10-14 | ||
| PCT/US2015/055034 WO2016060963A1 (en) | 2014-10-14 | 2015-10-10 | Substituted heteroaryl compounds and methods of use |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2017531000A JP2017531000A (ja) | 2017-10-19 |
| JP2017531000A5 true JP2017531000A5 (enExample) | 2018-11-01 |
| JP6649540B2 JP6649540B2 (ja) | 2020-02-19 |
Family
ID=55747172
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2017519817A Active JP6649540B2 (ja) | 2014-10-14 | 2015-10-10 | 置換されたヘテロアリール化合物および使用方法 |
Country Status (6)
| Country | Link |
|---|---|
| US (1) | US10059689B2 (enExample) |
| EP (1) | EP3206691B1 (enExample) |
| JP (1) | JP6649540B2 (enExample) |
| ES (1) | ES2699948T3 (enExample) |
| TW (1) | TW201617338A (enExample) |
| WO (1) | WO2016060963A1 (enExample) |
Families Citing this family (18)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP3347097B1 (en) | 2015-09-11 | 2021-02-24 | Sunshine Lake Pharma Co., Ltd. | Substituted aminopyrimidine derivatives as modulators of the kinases jak, flt3 and aurora |
| BR102018007822A2 (pt) | 2017-04-20 | 2018-11-06 | Gilead Sciences, Inc. | composto, métodos para inibir pd-1, pd-l1 e/ou interação de pd-1/pd-l1 e para tratamento de câncer, composição farmacêutica, e, kit para tratamento de ou prevenção de câncer ou uma doença ou condição |
| CN109776522B (zh) * | 2017-10-30 | 2020-12-29 | 广东东阳光药业有限公司 | 取代的杂芳基化合物及其组合物和用途 |
| WO2019099311A1 (en) | 2017-11-19 | 2019-05-23 | Sunshine Lake Pharma Co., Ltd. | Substituted heteroaryl compounds and methods of use |
| KR102708681B1 (ko) | 2018-02-13 | 2024-09-26 | 길리애드 사이언시즈, 인코포레이티드 | Pd-1/pd-l1 억제제 |
| EP4600247A3 (en) | 2018-04-19 | 2025-11-19 | Gilead Sciences, Inc. | Pd-1/pd-l1 inhibitors |
| UA126421C2 (uk) | 2018-07-13 | 2022-09-28 | Гіліад Сайєнсіз, Інк. | Інгібітори pd-1/pd-l1 |
| US11236085B2 (en) | 2018-10-24 | 2022-02-01 | Gilead Sciences, Inc. | PD-1/PD-L1 inhibitors |
| EP3876939A4 (en) | 2018-11-07 | 2022-08-10 | Dana-Farber Cancer Institute, Inc. | Benzothiazole derivatives and 7-aza-benzothiazole derivatives as janus kinase 2 inhibitors and uses thereof |
| EP3876930A4 (en) | 2018-11-07 | 2022-07-20 | Dana-Farber Cancer Institute, Inc. | BENZIMIDAZOLE DERIVATIVES AND AZA-BENZIMIDAZOLE DERIVATIVES AS JANUS KINASE 2 INHIBITORS AND USES THEREOF |
| WO2020097400A1 (en) | 2018-11-07 | 2020-05-14 | Dana-Farber Cancer Institute, Inc. | Imidazopyridine derivatives and aza-imidazopyridine derivatives as janus kinase 2 inhibitors and uses thereof |
| US12157730B2 (en) | 2019-03-19 | 2024-12-03 | Voronoi Inc. | Heteroaryl derivative, method for producing same, and pharmaceutical composition comprising same as effective component |
| AU2020240382B2 (en) * | 2019-03-19 | 2022-08-25 | Voronoi Inc. | Heteroaryl derivative, method for producing same, and pharmaceutical composition comprising same as effective component |
| WO2021083185A1 (zh) * | 2019-10-29 | 2021-05-06 | 沈阳中化农药化工研发有限公司 | 含嘧啶的哌啶胺类化合物及其制备方法和用途 |
| BR112022022409A2 (pt) | 2020-05-06 | 2023-02-07 | Ajax Therapeutics Inc | 6-heteroarilóxi benzimidazóis e azabenzimidazóis como inibidores de jak2 |
| WO2022140527A1 (en) | 2020-12-23 | 2022-06-30 | Ajax Therapeutics, Inc. | 6-heteroaryloxy benzimidazoles and azabenzimidazoles as jak2 inhibitors |
| CA3234638A1 (en) | 2021-11-09 | 2023-05-19 | Ajax Therapeutics, Inc. | 6-heteroaryloxy benzimidazoles and azabenzimidazoles as jak2 inhibitors |
| WO2023086320A1 (en) | 2021-11-09 | 2023-05-19 | Ajax Therapeutics, Inc. | Forms and compositions of inhibitors of jak2 |
Family Cites Families (33)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DE69933680T2 (de) * | 1998-08-29 | 2007-08-23 | Astrazeneca Ab | Pyrimidine verbindungen |
| WO2003030909A1 (en) | 2001-09-25 | 2003-04-17 | Bayer Pharmaceuticals Corporation | 2- and 4-aminopyrimidines n-substtituded by a bicyclic ring for use as kinase inhibitors in the treatment of cancer |
| TWI329105B (en) | 2002-02-01 | 2010-08-21 | Rigel Pharmaceuticals Inc | 2,4-pyrimidinediamine compounds and their uses |
| WO2004037814A1 (en) | 2002-10-25 | 2004-05-06 | Vertex Pharmaceuticals Incorporated | Indazolinone compositions useful as kinase inhibitors |
| US7754714B2 (en) | 2004-05-18 | 2010-07-13 | Rigel Pharmaceuticals, Inc. | Cycloalkyl substituted pyrimidinediamine compounds and their uses |
| GB2420559B (en) | 2004-11-15 | 2008-08-06 | Rigel Pharmaceuticals Inc | Stereoisomerically enriched 3-aminocarbonyl bicycloheptene pyrimidinediamine compounds and their uses |
| WO2006067614A2 (en) | 2004-12-23 | 2006-06-29 | Pfizer Products Inc. | Heteroaromatic derivatives useful as anticancer agents |
| CA2590110C (en) * | 2004-12-30 | 2014-06-03 | Exelixis, Inc. | Kinase modulators and method of use |
| EP2054392A2 (en) * | 2006-06-15 | 2009-05-06 | Boehringer Ingelheim International GmbH | 2-anilino-4-(heterocyclic)amino-pyrimidines as inhibitors of protein kinase c-alpha |
| US7947698B2 (en) | 2007-03-23 | 2011-05-24 | Rigel Pharmaceuticals, Inc. | Compositions and methods for inhibition of the JAK pathway |
| CN101903357A (zh) | 2007-07-17 | 2010-12-01 | 里格尔药品股份有限公司 | 作为pkc抑制剂的环状胺取代的嘧啶二胺 |
| US8138339B2 (en) | 2008-04-16 | 2012-03-20 | Portola Pharmaceuticals, Inc. | Inhibitors of protein kinases |
| JP5705720B2 (ja) * | 2008-04-16 | 2015-04-22 | ポートラ ファーマシューティカルズ， インコーポレイテッド | Ｓｙｋまたはｊａｋキナーゼ阻害剤としての２，６−ジアミノ−ピリミジン−５−イル−カルボキサミド |
| US8338439B2 (en) | 2008-06-27 | 2012-12-25 | Celgene Avilomics Research, Inc. | 2,4-disubstituted pyrimidines useful as kinase inhibitors |
| NZ603525A (en) | 2008-06-27 | 2015-02-27 | Celgene Avilomics Res Inc | Pyrimidine based compound and uses thereof |
| JPWO2010058846A1 (ja) * | 2008-11-21 | 2012-04-19 | アステラス製薬株式会社 | ４，６−ジアミノニコチンアミド化合物 |
| US8268851B2 (en) * | 2008-12-23 | 2012-09-18 | Rigel Pharmaceuticals, Inc. | Compositions and methods for inhibition of the JAK pathway |
| ES2635504T3 (es) | 2009-01-21 | 2017-10-04 | Rigel Pharmaceuticals, Inc. | Derivados de N2-(3-piridilo o fenil)-N4-(4-piperidil)-2,4-pirimidinadiamina útiles en el tratamiento de enfermedades inflamatorias, toimmunitarias o proliferativas |
| JP5918693B2 (ja) * | 2009-05-05 | 2016-05-18 | ダナ ファーバー キャンサー インスティテュート インコーポレイテッド | Ｅｇｆｒ阻害剤及び疾患の治療方法 |
| CN102498110A (zh) | 2009-06-10 | 2012-06-13 | 雅培制药有限公司 | 作为激酶抑制剂的2-(lh-吡唑-4-基氨基)-嘧啶 |
| US20110130415A1 (en) | 2009-12-01 | 2011-06-02 | Rajinder Singh | Protein kinase c inhibitors and uses thereof |
| JP6035238B2 (ja) | 2010-07-21 | 2016-11-30 | ライジェル ファーマシューティカルズ， インコーポレイテッド | プロテインキナーゼｃ阻害剤およびその使用 |
| CA2816219C (en) | 2010-11-01 | 2019-10-29 | Portola Pharmaceuticals, Inc. | Nicotinamides as syk modulators |
| SI2638031T1 (en) | 2010-11-10 | 2018-02-28 | Genentech, Inc. | Pyrazole aminopyrimidine derivatives as LRRK2 modulators |
| EP2710003A1 (en) * | 2011-05-16 | 2014-03-26 | OSI Pharmaceuticals, LLC | Fused bicyclic kinase inhibitors |
| HUE048834T2 (hu) * | 2011-05-17 | 2020-08-28 | Univ California | Kináz inhibitorok |
| EP2554544A1 (en) * | 2011-08-01 | 2013-02-06 | Almirall, S.A. | Pyridin-2(1h)-one derivatives as jak inhibitors |
| CN103159742B (zh) | 2011-12-16 | 2015-08-12 | 北京韩美药品有限公司 | 5-氯嘧啶类化合物及其作为egfr酪氨酸激酶抑制剂的应用 |
| WO2013152198A1 (en) | 2012-04-04 | 2013-10-10 | Rigel Pharmaceuticals, Inc. | Protein kinase c inhibitors and uses thereof |
| WO2015025197A1 (en) | 2013-08-22 | 2015-02-26 | Jubilant Biosys Limited | Substituted pyrimidine compounds, compositions and medicinal applications thereof |
| CN104262328B (zh) | 2013-09-18 | 2016-09-07 | 北京韩美药品有限公司 | 抑制btk和/或jak3激酶活性的化合物 |
| KR20160063366A (ko) | 2013-10-21 | 2016-06-03 | 메르크 파텐트 게엠베하 | Btk 저해제로서 헤테로아릴 화합물 및 이들의 용도 |
| CN105461694B (zh) * | 2014-09-27 | 2019-05-24 | 广东东阳光药业有限公司 | 取代的杂芳基化合物及其组合物和用途 |
-
2015
- 2015-10-10 EP EP15851260.8A patent/EP3206691B1/en active Active
- 2015-10-10 JP JP2017519817A patent/JP6649540B2/ja active Active
- 2015-10-10 WO PCT/US2015/055034 patent/WO2016060963A1/en not_active Ceased
- 2015-10-10 ES ES15851260T patent/ES2699948T3/es active Active
- 2015-10-10 US US14/880,199 patent/US10059689B2/en active Active
- 2015-10-12 TW TW104133416A patent/TW201617338A/zh unknown
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