JP2015526519A5 - - Google Patents
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- Publication number
- JP2015526519A5 JP2015526519A5 JP2015529957A JP2015529957A JP2015526519A5 JP 2015526519 A5 JP2015526519 A5 JP 2015526519A5 JP 2015529957 A JP2015529957 A JP 2015529957A JP 2015529957 A JP2015529957 A JP 2015529957A JP 2015526519 A5 JP2015526519 A5 JP 2015526519A5
- Authority
- JP
- Japan
- Prior art keywords
- alkyl
- cancer
- compound according
- composition
- pharmaceutically acceptable
- 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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- 150000001875 compounds Chemical class 0.000 claims description 65
- 125000000217 alkyl group Chemical group 0.000 claims description 45
- -1 2-oxa-bicyclo [2.2.1] heptan-5-yl Chemical group 0.000 claims description 37
- 150000003839 salts Chemical class 0.000 claims description 22
- 229910052736 halogen Inorganic materials 0.000 claims description 20
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims description 20
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims description 20
- 125000001072 heteroaryl group Chemical group 0.000 claims description 19
- 125000003545 alkoxy group Chemical group 0.000 claims description 18
- 206010028980 Neoplasm Diseases 0.000 claims description 16
- 201000011510 cancer Diseases 0.000 claims description 16
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims description 16
- 150000002367 halogens Chemical class 0.000 claims description 16
- 230000003463 hyperproliferative effect Effects 0.000 claims description 16
- 125000000623 heterocyclic group Chemical group 0.000 claims description 15
- 208000035475 disorder Diseases 0.000 claims description 12
- 125000003226 pyrazolyl group Chemical group 0.000 claims description 10
- 238000000034 method Methods 0.000 claims description 9
- 125000002768 hydroxyalkyl group Chemical group 0.000 claims description 8
- 125000004076 pyridyl group Chemical group 0.000 claims description 8
- 125000004737 (C1-C6) haloalkoxy group Chemical group 0.000 claims description 6
- 125000000171 (C1-C6) haloalkyl group Chemical group 0.000 claims description 6
- 102100024193 Mitogen-activated protein kinase 1 Human genes 0.000 claims description 6
- 125000004093 cyano group Chemical group *C#N 0.000 claims description 6
- 230000000694 effects Effects 0.000 claims description 6
- 125000005843 halogen group Chemical group 0.000 claims description 6
- 230000002401 inhibitory effect Effects 0.000 claims description 5
- 239000008194 pharmaceutical composition Substances 0.000 claims description 5
- 125000004191 (C1-C6) alkoxy group Chemical group 0.000 claims description 4
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 claims description 4
- 125000006272 (C3-C7) cycloalkyl group Chemical group 0.000 claims description 4
- 125000006570 (C5-C6) heteroaryl group Chemical group 0.000 claims description 4
- 206010006187 Breast cancer Diseases 0.000 claims description 4
- 208000026310 Breast neoplasm Diseases 0.000 claims description 4
- 206010009944 Colon cancer Diseases 0.000 claims description 4
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims description 4
- 206010058467 Lung neoplasm malignant Diseases 0.000 claims description 4
- 206010033128 Ovarian cancer Diseases 0.000 claims description 4
- 206010061535 Ovarian neoplasm Diseases 0.000 claims description 4
- 208000024770 Thyroid neoplasm Diseases 0.000 claims description 4
- 125000003118 aryl group Chemical group 0.000 claims description 4
- 125000001797 benzyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])* 0.000 claims description 4
- 201000010099 disease Diseases 0.000 claims description 4
- 239000003814 drug Substances 0.000 claims description 4
- 125000005842 heteroatom Chemical group 0.000 claims description 4
- 229910052739 hydrogen Inorganic materials 0.000 claims description 4
- 239000001257 hydrogen Substances 0.000 claims description 4
- 201000005202 lung cancer Diseases 0.000 claims description 4
- 208000020816 lung neoplasm Diseases 0.000 claims description 4
- 125000000951 phenoxy group Chemical group [H]C1=C([H])C([H])=C(O*)C([H])=C1[H] 0.000 claims description 4
- 125000000719 pyrrolidinyl group Chemical group 0.000 claims description 4
- 125000001412 tetrahydropyranyl group Chemical group 0.000 claims description 4
- 201000002510 thyroid cancer Diseases 0.000 claims description 4
- 239000003085 diluting agent Substances 0.000 claims description 3
- 239000003937 drug carrier Substances 0.000 claims description 3
- 239000000546 pharmaceutical excipient Substances 0.000 claims description 3
- 125000003718 tetrahydrofuranyl group Chemical group 0.000 claims description 3
- 125000006273 (C1-C3) alkyl group Chemical group 0.000 claims description 2
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 claims description 2
- 125000006700 (C1-C6) alkylthio group Chemical group 0.000 claims description 2
- 125000006728 (C1-C6) alkynyl group Chemical group 0.000 claims description 2
- 125000004180 3-fluorophenyl group Chemical group [H]C1=C([H])C(*)=C([H])C(F)=C1[H] 0.000 claims description 2
- 125000004195 4-methylpiperazin-1-yl group Chemical group [H]C([H])([H])N1C([H])([H])C([H])([H])N(*)C([H])([H])C1([H])[H] 0.000 claims description 2
- 125000004863 4-trifluoromethoxyphenyl group Chemical group [H]C1=C([H])C(OC(F)(F)F)=C([H])C([H])=C1* 0.000 claims description 2
- 208000031261 Acute myeloid leukaemia Diseases 0.000 claims description 2
- 208000010507 Adenocarcinoma of Lung Diseases 0.000 claims description 2
- 208000003200 Adenoma Diseases 0.000 claims description 2
- 206010001233 Adenoma benign Diseases 0.000 claims description 2
- 208000032791 BCR-ABL1 positive chronic myelogenous leukemia Diseases 0.000 claims description 2
- 206010005003 Bladder cancer Diseases 0.000 claims description 2
- 208000003174 Brain Neoplasms Diseases 0.000 claims description 2
- 208000010833 Chronic myeloid leukaemia Diseases 0.000 claims description 2
- 208000001333 Colorectal Neoplasms Diseases 0.000 claims description 2
- 208000017604 Hodgkin disease Diseases 0.000 claims description 2
- 208000010747 Hodgkins lymphoma Diseases 0.000 claims description 2
- 208000008839 Kidney Neoplasms Diseases 0.000 claims description 2
- 208000034578 Multiple myelomas Diseases 0.000 claims description 2
- 201000003793 Myelodysplastic syndrome Diseases 0.000 claims description 2
- 208000033761 Myelogenous Chronic BCR-ABL Positive Leukemia Diseases 0.000 claims description 2
- 208000033776 Myeloid Acute Leukemia Diseases 0.000 claims description 2
- 208000033833 Myelomonocytic Chronic Leukemia Diseases 0.000 claims description 2
- 206010029260 Neuroblastoma Diseases 0.000 claims description 2
- 208000015914 Non-Hodgkin lymphomas Diseases 0.000 claims description 2
- 206010061902 Pancreatic neoplasm Diseases 0.000 claims description 2
- 206010035226 Plasma cell myeloma Diseases 0.000 claims description 2
- 206010060862 Prostate cancer Diseases 0.000 claims description 2
- 208000000236 Prostatic Neoplasms Diseases 0.000 claims description 2
- 208000015634 Rectal Neoplasms Diseases 0.000 claims description 2
- 206010038389 Renal cancer Diseases 0.000 claims description 2
- 206010039491 Sarcoma Diseases 0.000 claims description 2
- 208000024313 Testicular Neoplasms Diseases 0.000 claims description 2
- 206010057644 Testis cancer Diseases 0.000 claims description 2
- 208000007097 Urinary Bladder Neoplasms Diseases 0.000 claims description 2
- 239000002246 antineoplastic agent Substances 0.000 claims description 2
- 201000010902 chronic myelomonocytic leukemia Diseases 0.000 claims description 2
- 208000029742 colonic neoplasm Diseases 0.000 claims description 2
- 125000000753 cycloalkyl group Chemical group 0.000 claims description 2
- 229940127089 cytotoxic agent Drugs 0.000 claims description 2
- 210000002615 epidermis Anatomy 0.000 claims description 2
- 230000003325 follicular Effects 0.000 claims description 2
- 208000005017 glioblastoma Diseases 0.000 claims description 2
- 201000010536 head and neck cancer Diseases 0.000 claims description 2
- 208000014829 head and neck neoplasm Diseases 0.000 claims description 2
- 125000002883 imidazolyl group Chemical group 0.000 claims description 2
- 125000001041 indolyl group Chemical group 0.000 claims description 2
- 201000010982 kidney cancer Diseases 0.000 claims description 2
- 208000003849 large cell carcinoma Diseases 0.000 claims description 2
- 208000032839 leukemia Diseases 0.000 claims description 2
- 201000007270 liver cancer Diseases 0.000 claims description 2
- 208000014018 liver neoplasm Diseases 0.000 claims description 2
- 201000005249 lung adenocarcinoma Diseases 0.000 claims description 2
- 208000015486 malignant pancreatic neoplasm Diseases 0.000 claims description 2
- 238000004519 manufacturing process Methods 0.000 claims description 2
- 201000001441 melanoma Diseases 0.000 claims description 2
- 208000025113 myeloid leukemia Diseases 0.000 claims description 2
- 125000003566 oxetanyl group Chemical group 0.000 claims description 2
- 210000000496 pancreas Anatomy 0.000 claims description 2
- 201000002528 pancreatic cancer Diseases 0.000 claims description 2
- 208000008443 pancreatic carcinoma Diseases 0.000 claims description 2
- 125000003386 piperidinyl group Chemical group 0.000 claims description 2
- 125000003373 pyrazinyl group Chemical group 0.000 claims description 2
- 125000002098 pyridazinyl group Chemical group 0.000 claims description 2
- 125000000714 pyrimidinyl group Chemical group 0.000 claims description 2
- 206010038038 rectal cancer Diseases 0.000 claims description 2
- 201000001275 rectum cancer Diseases 0.000 claims description 2
- 201000000849 skin cancer Diseases 0.000 claims description 2
- 208000000649 small cell carcinoma Diseases 0.000 claims description 2
- 201000003120 testicular cancer Diseases 0.000 claims description 2
- 238000002560 therapeutic procedure Methods 0.000 claims description 2
- 201000005112 urinary bladder cancer Diseases 0.000 claims description 2
- 239000000203 mixture Substances 0.000 claims 21
- WYURNTSHIVDZCO-UHFFFAOYSA-N Tetrahydrofuran Chemical compound C1CCOC1 WYURNTSHIVDZCO-UHFFFAOYSA-N 0.000 description 2
- YLQBMQCUIZJEEH-UHFFFAOYSA-N tetrahydrofuran Natural products C=1C=COC=1 YLQBMQCUIZJEEH-UHFFFAOYSA-N 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201261693671P | 2012-08-27 | 2012-08-27 | |
| US61/693,671 | 2012-08-27 | ||
| PCT/US2013/056876 WO2014036015A1 (en) | 2012-08-27 | 2013-08-27 | Serine/threonine kinase inhibitors for the treatment of hyperproliferative|diseases |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2015526519A JP2015526519A (ja) | 2015-09-10 |
| JP2015526519A5 true JP2015526519A5 (https=) | 2016-10-13 |
| JP6378182B2 JP6378182B2 (ja) | 2018-08-22 |
Family
ID=49118823
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2015529957A Active JP6378182B2 (ja) | 2012-08-27 | 2013-08-27 | 過剰増殖性│疾患の処置のためのセリン／スレオニンキナーゼ阻害剤 |
Country Status (13)
| Country | Link |
|---|---|
| US (1) | US9388171B2 (https=) |
| EP (1) | EP2888247B1 (https=) |
| JP (1) | JP6378182B2 (https=) |
| KR (1) | KR20150047597A (https=) |
| CN (1) | CN105143200B (https=) |
| AR (1) | AR092253A1 (https=) |
| BR (1) | BR112015004548A2 (https=) |
| CA (1) | CA2882750A1 (https=) |
| HK (1) | HK1210174A1 (https=) |
| MX (1) | MX369989B (https=) |
| RU (1) | RU2644947C2 (https=) |
| TW (1) | TW201408658A (https=) |
| WO (1) | WO2014036015A1 (https=) |
Families Citing this family (23)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP2681215B1 (en) | 2011-02-28 | 2015-04-22 | Array Biopharma, Inc. | Serine/threonine kinase inhibitors |
| US9187462B2 (en) | 2011-08-04 | 2015-11-17 | Array Biopharma Inc. | Substituted quinazolines as serine/threonine kinase inhibitors |
| DK2820009T3 (en) | 2012-03-01 | 2018-04-16 | Array Biopharma Inc | Serine / threonine kinase inhibitors |
| TWI616430B (zh) * | 2012-07-27 | 2018-03-01 | 百健Ｍａ公司 | Ａｔｘ調節劑 |
| MX2015004615A (es) | 2012-10-16 | 2015-07-17 | Hoffmann La Roche | Inhibidores de serina/treonina cinasa. |
| US9532987B2 (en) | 2013-09-05 | 2017-01-03 | Genentech, Inc. | Use of a combination of a MEK inhibitor and an ERK inhibitor for treatment of hyperproliferative diseases |
| CN106029672B (zh) | 2013-12-06 | 2019-03-29 | 基因泰克公司 | 丝氨酸/苏氨酸激酶抑制剂 |
| JP6642942B2 (ja) | 2013-12-30 | 2020-02-12 | アレイ バイオファーマ、インコーポレイテッド | セリン／トレオニンキナーゼ阻害剤 |
| BR112016015235A2 (pt) | 2013-12-30 | 2017-08-08 | Genentech Inc | Composto, composição farmacêutica, método de inibição da atividade da proteína quinase erk e método de tratamento |
| US9879029B2 (en) * | 2014-12-22 | 2018-01-30 | Eli Lilly And Company | ERK inhibitors |
| KR20180134347A (ko) | 2016-04-15 | 2018-12-18 | 제넨테크, 인크. | 암의 진단 및 치료 방법 |
| CN106749117B (zh) * | 2016-11-29 | 2018-10-09 | 北京怡力生物科技有限公司 | 一种3-氨基甲基四氢呋喃的制备方法 |
| EP3601259B1 (en) | 2017-03-30 | 2022-02-23 | F. Hoffmann-La Roche AG | Isoquinolines as inhibitors of hpk1 |
| EP3640242B1 (en) * | 2017-06-16 | 2023-04-19 | Hitgen Ltd. | Rock-inhibiting compound and uses thereof |
| KR102811888B1 (ko) | 2017-09-08 | 2025-05-27 | 에프. 호프만-라 로슈 아게 | 암의 진단 및 치료 방법 |
| EP3752200A1 (en) | 2018-02-13 | 2020-12-23 | Vib Vzw | Targeting minimal residual disease in cancer with rxr antagonists |
| CN108558869B (zh) * | 2018-05-10 | 2019-04-09 | 西安培华学院 | 用于治疗肝癌的化合物及其制剂 |
| TW202019905A (zh) | 2018-07-24 | 2020-06-01 | 瑞士商赫孚孟拉羅股份公司 | 異喹啉化合物及其用途 |
| TW202024053A (zh) | 2018-10-02 | 2020-07-01 | 美商建南德克公司 | 異喹啉化合物及其用途 |
| US11612606B2 (en) | 2018-10-03 | 2023-03-28 | Genentech, Inc. | 8-aminoisoquinoline compounds and uses thereof |
| CU20210080A7 (es) | 2019-04-02 | 2022-05-11 | Array Biopharma Inc | Triazinas sustituidas como inhibidores de proteína tirosina fosfatasa |
| US20220389009A1 (en) * | 2019-10-01 | 2022-12-08 | Goldfinch Bio, Inc. | Substituted 1,6-naphthyridine inhibitors of cdk5 |
| US12570640B2 (en) | 2020-09-02 | 2026-03-10 | Merck Sharp & Dohme Llc | 2-aminoquinazolines as LRRK2 inhibitors, pharmaceutical compositions, and uses thereof |
Family Cites Families (36)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO1995009847A1 (en) | 1993-10-01 | 1995-04-13 | Ciba-Geigy Ag | Pyrimidineamine derivatives and processes for the preparation thereof |
| WO1995009851A1 (en) | 1993-10-01 | 1995-04-13 | Ciba-Geigy Ag | Pharmacologically active pyrimidineamine derivatives and processes for the preparation thereof |
| US5543523A (en) | 1994-11-15 | 1996-08-06 | Regents Of The University Of Minnesota | Method and intermediates for the synthesis of korupensamines |
| EP0948496A2 (en) | 1996-12-05 | 1999-10-13 | Amgen inc. | Substituted pyrimidinone and pyridone compounds and methods of use |
| GB9812683D0 (en) * | 1998-06-12 | 1998-08-12 | Smithkline Beecham Plc | Novel compounds |
| US6602872B1 (en) | 1999-12-13 | 2003-08-05 | Merck & Co., Inc. | Substituted pyridazines having cytokine inhibitory activity |
| WO2001062233A2 (en) | 2000-02-25 | 2001-08-30 | F. Hoffmann La Roche Ag | Adenosine receptor modulators |
| AU5260601A (en) | 2000-04-26 | 2001-11-07 | Eisai Co Ltd | Medicinal compositions promoting bowel movement |
| WO2002088079A2 (en) | 2001-05-01 | 2002-11-07 | Bristol-Myers Squibb Company | Dual inhibitors of pde 7 and pde 4 |
| 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 |
| JP4606161B2 (ja) | 2002-05-21 | 2011-01-05 | アムジエン・インコーポレーテツド | 置換複素環式化合物および使用方法 |
| US7208498B2 (en) | 2002-07-15 | 2007-04-24 | Merck & Co., Inc. | Piperidino pyrimidine dipeptidyl peptidase inhibitors for the treatment of diabetes |
| TW200533357A (en) | 2004-01-08 | 2005-10-16 | Millennium Pharm Inc | 2-(amino-substituted)-4-aryl pyrimidines and related compounds useful for treating inflammatory diseases |
| CA2561895A1 (en) | 2004-04-13 | 2005-10-27 | Icagen, Inc. | Polycyclic pyrimidines as potassium ion channel modulators |
| US7429604B2 (en) | 2004-06-15 | 2008-09-30 | Bristol Myers Squibb Company | Six-membered heterocycles useful as serine protease inhibitors |
| JP2008510766A (ja) | 2004-08-27 | 2008-04-10 | ゲーペーツェー ビオテック アーゲー | ピリミジン誘導体 |
| GB0420722D0 (en) | 2004-09-17 | 2004-10-20 | Addex Pharmaceuticals Sa | Novel allosteric modulators |
| GB0428514D0 (en) | 2004-12-31 | 2005-02-09 | Prosidion Ltd | Compounds |
| TW200716594A (en) | 2005-04-18 | 2007-05-01 | Neurogen Corp | Substituted heteroaryl CB1 antagonists |
| US7572809B2 (en) * | 2005-12-19 | 2009-08-11 | Hoffmann-La Roche Inc. | Isoquinoline aminopyrazole derivatives |
| JP2009528280A (ja) | 2006-02-16 | 2009-08-06 | シェーリング コーポレイション | Ｅｒｋインヒビターとしてのピロリジン誘導体 |
| CA2651072A1 (en) | 2006-05-01 | 2007-11-08 | Pfizer Products Inc. | Substituted 2-amino-fused heterocyclic compounds |
| DE102006035202A1 (de) | 2006-07-29 | 2008-01-31 | Lanxess Deutschland Gmbh | Konservierungsmittel auf Basis von Carbonsäureanhydriden |
| TWI389899B (zh) * | 2006-08-08 | 2013-03-21 | Msd Oss Bv | 具口服活性之凝血酶抑制劑 |
| CN101528729A (zh) | 2006-08-23 | 2009-09-09 | 辉瑞产品公司 | 作为gsk-3抑制剂的嘧啶酮化合物 |
| WO2008039882A1 (en) | 2006-09-30 | 2008-04-03 | Sanofi-Aventis U.S. Llc | A combination of niacin and a prostaglandin d2 receptor antagonist |
| CN101568529A (zh) | 2006-12-22 | 2009-10-28 | 诺瓦提斯公司 | 作为cdk抑制剂、用于治疗癌症、炎症和病毒感染的杂芳基-杂芳基化合物 |
| JP5611826B2 (ja) | 2007-09-04 | 2014-10-22 | ザ スクリプス リサーチ インスティテュート | タンパク質キナーゼ阻害剤としての置換されたピリミジニル−アミン |
| AU2008324833A1 (en) | 2007-11-06 | 2009-05-14 | E. I. Du Pont De Nemours And Company | Fungicidal heterocyclic amines |
| WO2009146034A2 (en) | 2008-03-31 | 2009-12-03 | Takeda Pharmaceutical Company Limited | Mapk/erk kinase inhibitors and methods of use thereof |
| US9187426B2 (en) | 2008-06-27 | 2015-11-17 | Novartis Ag | Organic compounds |
| NZ603525A (en) | 2008-06-27 | 2015-02-27 | Celgene Avilomics Res Inc | Pyrimidine based compound and uses thereof |
| ES2548882T3 (es) | 2008-12-08 | 2015-10-21 | Arena Pharmaceuticals, Inc. | Moduladores del receptor de prostaciclina (PGl2) útiles para el tratamiento de trastornos relacionados con los mismos |
| EP2681215B1 (en) | 2011-02-28 | 2015-04-22 | Array Biopharma, Inc. | Serine/threonine kinase inhibitors |
| US9187462B2 (en) * | 2011-08-04 | 2015-11-17 | Array Biopharma Inc. | Substituted quinazolines as serine/threonine kinase inhibitors |
| DK2820009T3 (en) | 2012-03-01 | 2018-04-16 | Array Biopharma Inc | Serine / threonine kinase inhibitors |
-
2013
- 2013-08-27 TW TW102130680A patent/TW201408658A/zh unknown
- 2013-08-27 MX MX2015002508A patent/MX369989B/es active IP Right Grant
- 2013-08-27 CA CA2882750A patent/CA2882750A1/en not_active Abandoned
- 2013-08-27 HK HK15111084.7A patent/HK1210174A1/xx unknown
- 2013-08-27 AR ARP130103040A patent/AR092253A1/es unknown
- 2013-08-27 EP EP13759395.0A patent/EP2888247B1/en active Active
- 2013-08-27 JP JP2015529957A patent/JP6378182B2/ja active Active
- 2013-08-27 BR BR112015004548A patent/BR112015004548A2/pt not_active IP Right Cessation
- 2013-08-27 CN CN201380051518.1A patent/CN105143200B/zh active Active
- 2013-08-27 RU RU2015110985A patent/RU2644947C2/ru not_active IP Right Cessation
- 2013-08-27 KR KR1020157007729A patent/KR20150047597A/ko not_active Withdrawn
- 2013-08-27 WO PCT/US2013/056876 patent/WO2014036015A1/en not_active Ceased
- 2013-08-27 US US14/011,501 patent/US9388171B2/en active Active
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