JP2014500295A5 - - Google Patents
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- Publication number
- JP2014500295A5 JP2014500295A5 JP2013545375A JP2013545375A JP2014500295A5 JP 2014500295 A5 JP2014500295 A5 JP 2014500295A5 JP 2013545375 A JP2013545375 A JP 2013545375A JP 2013545375 A JP2013545375 A JP 2013545375A JP 2014500295 A5 JP2014500295 A5 JP 2014500295A5
- Authority
- JP
- Japan
- Prior art keywords
- alkyl
- independently
- ring system
- hydrogen
- membered
- 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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- 125000000217 alkyl group Chemical group 0.000 claims description 70
- 150000001875 compounds Chemical class 0.000 claims description 61
- 125000001424 substituent group Chemical group 0.000 claims description 44
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims description 39
- 229910052739 hydrogen Inorganic materials 0.000 claims description 36
- 239000001257 hydrogen Substances 0.000 claims description 36
- 125000000623 heterocyclic group Chemical group 0.000 claims description 34
- 125000004122 cyclic group Chemical group 0.000 claims description 27
- 125000003118 aryl group Chemical group 0.000 claims description 19
- 125000004093 cyano group Chemical group *C#N 0.000 claims description 19
- 229910052736 halogen Inorganic materials 0.000 claims description 18
- 150000002367 halogens Chemical class 0.000 claims description 18
- 125000001072 heteroaryl group Chemical group 0.000 claims description 17
- 125000006574 non-aromatic ring group Chemical group 0.000 claims description 16
- 150000003839 salts Chemical class 0.000 claims description 15
- 125000006376 (C3-C10) cycloalkyl group Chemical group 0.000 claims description 9
- 125000000882 C2-C6 alkenyl group Chemical group 0.000 claims description 9
- 125000003601 C2-C6 alkynyl group Chemical group 0.000 claims description 9
- 125000000392 cycloalkenyl group Chemical group 0.000 claims description 9
- 125000003545 alkoxy group Chemical group 0.000 claims description 8
- 239000013543 active substance Substances 0.000 claims description 7
- 125000000753 cycloalkyl group Chemical group 0.000 claims description 7
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims description 7
- 125000006570 (C5-C6) heteroaryl group Chemical group 0.000 claims description 6
- 229920006395 saturated elastomer Polymers 0.000 claims description 6
- 229910052799 carbon Inorganic materials 0.000 claims description 5
- 150000002431 hydrogen Chemical class 0.000 claims description 5
- 230000002265 prevention Effects 0.000 claims description 5
- 206010028980 Neoplasm Diseases 0.000 claims description 4
- 201000011510 cancer Diseases 0.000 claims description 4
- 239000003814 drug Substances 0.000 claims description 4
- 125000005647 linker group Chemical group 0.000 claims description 4
- 239000000825 pharmaceutical preparation Substances 0.000 claims description 4
- 125000004432 carbon atom Chemical group C* 0.000 claims description 3
- 229940079593 drug Drugs 0.000 claims description 3
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 claims description 3
- 125000004737 (C1-C6) haloalkoxy group Chemical group 0.000 claims description 2
- 125000000171 (C1-C6) haloalkyl group Chemical group 0.000 claims description 2
- 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 description 2
- 208000023275 Autoimmune disease Diseases 0.000 claims description 2
- 208000035473 Communicable disease Diseases 0.000 claims description 2
- 206010061218 Inflammation Diseases 0.000 claims description 2
- 230000032823 cell division Effects 0.000 claims description 2
- 231100000433 cytotoxic Toxicity 0.000 claims description 2
- 230000001472 cytotoxic effect Effects 0.000 claims description 2
- 125000001183 hydrocarbyl group Chemical group 0.000 claims description 2
- 208000015181 infectious disease Diseases 0.000 claims description 2
- 230000004054 inflammatory process Effects 0.000 claims description 2
- 230000002401 inhibitory effect Effects 0.000 claims description 2
- 239000000203 mixture Substances 0.000 claims description 2
- 239000008194 pharmaceutical composition Substances 0.000 claims 1
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 description 6
- WKBOTKDWSSQWDR-UHFFFAOYSA-N Bromine atom Chemical compound [Br] WKBOTKDWSSQWDR-UHFFFAOYSA-N 0.000 description 5
- FAPWRFPIFSIZLT-UHFFFAOYSA-M Sodium chloride Chemical compound [Na+].[Cl-] FAPWRFPIFSIZLT-UHFFFAOYSA-M 0.000 description 4
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 description 4
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 description 3
- -1 2,5-diaza-bicyclo [2,2,1] heptyl Chemical group 0.000 description 2
- 239000003708 ampul Substances 0.000 description 2
- 125000001301 ethoxy group Chemical group [H]C([H])([H])C([H])([H])O* 0.000 description 2
- 206010073071 hepatocellular carcinoma Diseases 0.000 description 2
- 231100000844 hepatocellular carcinoma Toxicity 0.000 description 2
- 125000000956 methoxy group Chemical group [H]C([H])([H])O* 0.000 description 2
- 208000002154 non-small cell lung carcinoma Diseases 0.000 description 2
- 239000011780 sodium chloride Substances 0.000 description 2
- 239000000243 solution Substances 0.000 description 2
- 208000029729 tumor suppressor gene on chromosome 11 Diseases 0.000 description 2
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Chemical compound O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 description 2
- 206010006187 Breast cancer Diseases 0.000 description 1
- 208000026310 Breast neoplasm Diseases 0.000 description 1
- ZAMOUSCENKQFHK-UHFFFAOYSA-N Chlorine atom Chemical compound [Cl] ZAMOUSCENKQFHK-UHFFFAOYSA-N 0.000 description 1
- 206010060862 Prostate cancer Diseases 0.000 description 1
- 208000000236 Prostatic Neoplasms Diseases 0.000 description 1
- 125000002947 alkylene group Chemical group 0.000 description 1
- GDTBXPJZTBHREO-UHFFFAOYSA-N bromine Substances BrBr GDTBXPJZTBHREO-UHFFFAOYSA-N 0.000 description 1
- 229910052794 bromium Inorganic materials 0.000 description 1
- 239000000969 carrier Substances 0.000 description 1
- 229910052801 chlorine Inorganic materials 0.000 description 1
- 239000000460 chlorine Substances 0.000 description 1
- 125000001559 cyclopropyl group Chemical group [H]C1([H])C([H])([H])C1([H])* 0.000 description 1
- 239000000706 filtrate Substances 0.000 description 1
- 230000004927 fusion Effects 0.000 description 1
- 125000001188 haloalkyl group Chemical group 0.000 description 1
- 238000000034 method Methods 0.000 description 1
- 125000002757 morpholinyl group Chemical group 0.000 description 1
- 239000000546 pharmaceutical excipient Substances 0.000 description 1
- 229940127557 pharmaceutical product Drugs 0.000 description 1
- 125000004193 piperazinyl group Chemical group 0.000 description 1
- 125000003386 piperidinyl group Chemical group 0.000 description 1
- 125000003226 pyrazolyl group Chemical group 0.000 description 1
- 125000004076 pyridyl group Chemical group 0.000 description 1
- 239000002510 pyrogen Substances 0.000 description 1
- 125000000719 pyrrolidinyl group Chemical group 0.000 description 1
- 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 description 1
- 239000008215 water for injection Substances 0.000 description 1
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP10196277.7 | 2010-12-21 | ||
| EP10196277 | 2010-12-21 | ||
| EP11189723 | 2011-11-18 | ||
| EP11189723.7 | 2011-11-18 | ||
| PCT/EP2011/073653 WO2012085126A1 (en) | 2010-12-21 | 2011-12-21 | Oxindolopyrimidine as igf1r receptor inhibitors |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2014500295A JP2014500295A (ja) | 2014-01-09 |
| JP2014500295A5 true JP2014500295A5 (enExample) | 2015-02-05 |
| JP5809288B2 JP5809288B2 (ja) | 2015-11-10 |
Family
ID=45507665
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2013545375A Active JP5809288B2 (ja) | 2010-12-21 | 2011-12-21 | Ｉｇｆ１ｒ受容体阻害薬としてのオキシインドールピリミジン |
Country Status (6)
| Country | Link |
|---|---|
| US (1) | US8546443B2 (enExample) |
| EP (1) | EP2655358B1 (enExample) |
| JP (1) | JP5809288B2 (enExample) |
| AR (1) | AR084444A1 (enExample) |
| UY (1) | UY33817A (enExample) |
| WO (1) | WO2012085126A1 (enExample) |
Families Citing this family (28)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US8765747B2 (en) | 2009-06-12 | 2014-07-01 | Dana-Farber Cancer Institute, Inc. | Fused 2-aminothiazole compounds |
| US8546443B2 (en) | 2010-12-21 | 2013-10-01 | Boehringer Ingelheim International Gmbh | Benzylic oxindole pyrimidines |
| US8889684B2 (en) | 2011-02-02 | 2014-11-18 | Boehringer Ingelheim International Gmbh | Azaindolylphenyl sulfonamides as serine/threonine kinase inhibitors |
| RS55701B1 (sr) | 2011-06-22 | 2017-07-31 | Purdue Pharma Lp | Trpv1 antagonisti koji uključuju dihidroksi supstituent i njihove upotrebe |
| JP6106685B2 (ja) | 2011-11-17 | 2017-04-05 | 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 | Ｃ−ｊｕｎ−ｎ−末端キナーゼ（ｊｎｋ）の阻害剤 |
| US9296725B2 (en) * | 2012-05-24 | 2016-03-29 | Cellzome Limited | Heterocyclyl pyrimidine analogues as TYK2 inhibitors |
| EP2909194A1 (en) | 2012-10-18 | 2015-08-26 | Dana-Farber Cancer Institute, Inc. | Inhibitors of cyclin-dependent kinase 7 (cdk7) |
| US10000483B2 (en) | 2012-10-19 | 2018-06-19 | Dana-Farber Cancer Institute, Inc. | Bone marrow on X chromosome kinase (BMX) inhibitors and uses thereof |
| USRE48175E1 (en) | 2012-10-19 | 2020-08-25 | Dana-Farber Cancer Institute, Inc. | Hydrophobically tagged small molecules as inducers of protein degradation |
| EP2959013A2 (en) | 2013-02-25 | 2015-12-30 | Novartis AG | Novel androgen receptor mutation |
| AU2014337044A1 (en) | 2013-10-18 | 2016-05-05 | Dana-Farber Cancer Institute, Inc. | Polycyclic inhibitors of cyclin-dependent kinase 7 (CDK7) |
| WO2015058126A1 (en) | 2013-10-18 | 2015-04-23 | Syros Pharmaceuticals, Inc. | Heteroaromatic compounds useful for the treatment of prolferative diseases |
| WO2015164614A1 (en) * | 2014-04-23 | 2015-10-29 | Dana-Farber Cancer Institute, Inc. | Janus kinase inhibitors and uses thereof |
| US9862688B2 (en) * | 2014-04-23 | 2018-01-09 | Dana-Farber Cancer Institute, Inc. | Hydrophobically tagged janus kinase inhibitors and uses thereof |
| US10870651B2 (en) | 2014-12-23 | 2020-12-22 | Dana-Farber Cancer Institute, Inc. | Inhibitors of cyclin-dependent kinase 7 (CDK7) |
| CN107427521B (zh) | 2015-03-27 | 2021-08-03 | 达纳-法伯癌症研究所股份有限公司 | 细胞周期蛋白依赖性激酶的抑制剂 |
| CA2986441A1 (en) | 2015-06-12 | 2016-12-15 | Dana-Farber Cancer Institute, Inc. | Combination therapy of transcription inhibitors and kinase inhibitors |
| WO2017044858A2 (en) | 2015-09-09 | 2017-03-16 | Dana-Farber Cancer Institute, Inc. | Inhibitors of cyclin-dependent kinases |
| EP3810132A4 (en) | 2018-06-25 | 2022-06-22 | Dana-Farber Cancer Institute, Inc. | TAIRE FAMILY KINASE INHIBITORS AND RELATED USES |
| US12509455B2 (en) | 2018-11-07 | 2025-12-30 | Dana-Farber Cancer Institute, Inc. | Imidazopyridine derivatives and aza-imidazopyridine derivatives as Janus kinase 2 inhibitors and uses thereof |
| 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 |
| WO2020097396A1 (en) | 2018-11-07 | 2020-05-14 | Dana-Farber Cancer Institute, Inc. | Benzimidazole derivatives and aza-benzimidazole derivatives as janus kinase 2 inhibitors and uses thereof |
| CN113164477A (zh) | 2018-12-14 | 2021-07-23 | 达纳-法伯癌症研究所股份有限公司 | C-jun-n-末端激酶的吡唑并吡啶抑制剂及其用途 |
| EP3902542A4 (en) | 2018-12-28 | 2022-09-07 | Dana-Farber Cancer Institute, Inc. | CYCLIN DEPENDENT KINASE 7 INHIBITORS AND USES THEREOF |
| JP2022545835A (ja) | 2019-08-28 | 2022-10-31 | ホライゾン セラピューティクス アイルランド デジグネイテッド アクティビティ カンパニー | 甲状腺眼症の治療方法 |
| CA3156828A1 (en) | 2019-10-03 | 2021-04-08 | Dana-Farber Cancer Institute, Inc. | Tricyclic kinase inhibitors and uses thereof |
| CN122003247A (zh) | 2023-07-07 | 2026-05-08 | 维里迪安治疗公司 | 治疗活动性和慢性甲状腺眼病的方法 |
| WO2025045203A1 (zh) * | 2023-09-01 | 2025-03-06 | 葆元生物医药科技(杭州)有限公司 | 杂环化合物及其中间体和应用 |
Family Cites Families (23)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US6525202B2 (en) | 2000-07-17 | 2003-02-25 | Wyeth | Cyclic amine phenyl beta-3 adrenergic receptor agonists |
| SE0104140D0 (sv) * | 2001-12-07 | 2001-12-07 | Astrazeneca Ab | Novel Compounds |
| WO2004048343A1 (en) * | 2002-11-28 | 2004-06-10 | Schering Aktiengesellschaft | Chk-, pdk- and akt-inhibitory pyrimidines, their production and use as pharmaceutical agents |
| UA80767C2 (en) * | 2002-12-20 | 2007-10-25 | Pfizer Prod Inc | Pyrimidine derivatives for the treatment of abnormal cell growth |
| GB0305929D0 (en) | 2003-03-14 | 2003-04-23 | Novartis Ag | Organic compounds |
| ATE542801T1 (de) | 2003-08-15 | 2012-02-15 | Novartis Ag | Zur behandlung von neoplastischen krankheiten, entzündlichen erkrankungen und erkrankungen des immunsystems geeignete 2,4-pyrimidindiamine |
| PL1663991T3 (pl) | 2003-09-05 | 2007-04-30 | Pfizer Prod Inc | Selektywna synteza CF3 – podstawionych pirymidyn |
| MXPA06013164A (es) * | 2004-05-14 | 2007-02-13 | Pfizer Prod Inc | Derivados de pirimidina para el tratamiento de crecimiento de celulas anormal. |
| US7521457B2 (en) | 2004-08-20 | 2009-04-21 | Boehringer Ingelheim International Gmbh | Pyrimidines as PLK inhibitors |
| WO2006021548A1 (de) | 2004-08-27 | 2006-03-02 | Boehringer Ingelheim International Gmbh | Dihydropteridinone, verfahren zu deren herstellung und deren verwendung als arzneimittel |
| GB0419161D0 (en) * | 2004-08-27 | 2004-09-29 | Novartis Ag | Organic compounds |
| US8211929B2 (en) * | 2004-12-30 | 2012-07-03 | Exelixis, Inc. | Pyrimidine derivatives as kinase modulators and method of use |
| DE102005016634A1 (de) * | 2005-04-12 | 2006-10-19 | Merck Patent Gmbh | Neuartige Aza-Hetercyclen als Kinase-Inhibitoren |
| WO2007081978A2 (en) | 2006-01-11 | 2007-07-19 | Angion Biomedica Corporation | Modulators of hepatocyte growth factor / c-met activity |
| EP2007754A1 (en) | 2006-04-10 | 2008-12-31 | Boehringer Ingelheim International GmbH | 2, 4-diaminopyrimidine derivatives and their use for the treatment of cancer |
| PE20080401A1 (es) | 2006-07-07 | 2008-06-23 | Boehringer Ingelheim Int | DERIVADOS DE HETEROARIL-FENIL SUSTITUIDOS COMO INHIBIDORES DE B-Raf-QUINASAS |
| BRPI0811898A2 (pt) | 2007-06-01 | 2019-09-24 | Glaxosmithkline Llc | composto, composição farmacêutica, métodos para tratar um neoplasma suscetível e um câncer em um mamífero, processo para preparar um composto, e, uso de um composto. |
| CL2008001943A1 (es) | 2007-07-02 | 2009-09-11 | Boehringer Ingelheim Int | Compuestos derivados de fenil-triazol, inhibidores de enzimas de señales especificas que participan del control de la proliferacion celular; composicion farmaceutica que comprende a dichos compuestos; y su uso para tratar cancer, infecciones, enfermedades inflamatorias y autoinmunes. |
| CA2692379A1 (en) | 2007-07-02 | 2009-01-08 | Boehringer Ingelheim International Gmbh | Antiproliferative compounds based on 5-membered heterocycles |
| US8461147B2 (en) * | 2007-12-03 | 2013-06-11 | Boehringer Ingelheim International Gmbh | Diaminopyridines for the treatment of diseases which are characterised by excessive or anomal cell proliferation |
| TW201024281A (en) * | 2008-11-24 | 2010-07-01 | Boehringer Ingelheim Int | New compounds |
| US9290507B2 (en) | 2010-03-26 | 2016-03-22 | Boehringer Ingelheim International Gmbh | B-RAF kinase inhibitors |
| US8546443B2 (en) | 2010-12-21 | 2013-10-01 | Boehringer Ingelheim International Gmbh | Benzylic oxindole pyrimidines |
-
2011
- 2011-12-19 US US13/329,615 patent/US8546443B2/en active Active
- 2011-12-19 UY UY0001033817A patent/UY33817A/es not_active Application Discontinuation
- 2011-12-20 AR ARP110104829A patent/AR084444A1/es unknown
- 2011-12-21 WO PCT/EP2011/073653 patent/WO2012085126A1/en not_active Ceased
- 2011-12-21 JP JP2013545375A patent/JP5809288B2/ja active Active
- 2011-12-21 EP EP11810833.1A patent/EP2655358B1/en active Active