JP2013532726A5 - - Google Patents
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- Publication number
- JP2013532726A5 JP2013532726A5 JP2013523206A JP2013523206A JP2013532726A5 JP 2013532726 A5 JP2013532726 A5 JP 2013532726A5 JP 2013523206 A JP2013523206 A JP 2013523206A JP 2013523206 A JP2013523206 A JP 2013523206A JP 2013532726 A5 JP2013532726 A5 JP 2013532726A5
- Authority
- JP
- Japan
- Prior art keywords
- alkyl
- alkylene
- pharmaceutically acceptable
- acceptable salt
- tautomer
- 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 description 305
- 150000003839 salts Chemical class 0.000 claims description 143
- 239000000203 mixture Substances 0.000 claims description 79
- 150000001875 compounds Chemical class 0.000 claims description 64
- 125000000623 heterocyclic group Chemical group 0.000 claims description 51
- 125000000753 cycloalkyl group Chemical group 0.000 claims description 38
- 125000005842 heteroatom Chemical group 0.000 claims description 32
- 125000003342 alkenyl group Chemical group 0.000 claims description 26
- 125000001424 substituent group Chemical group 0.000 claims description 26
- 206010028980 Neoplasm Diseases 0.000 claims description 24
- 125000000304 alkynyl group Chemical group 0.000 claims description 24
- 201000011510 cancer Diseases 0.000 claims description 24
- 125000003118 aryl group Chemical group 0.000 claims description 21
- -1 —I Chemical group 0.000 claims description 18
- 125000001313 C5-C10 heteroaryl group Chemical group 0.000 claims description 16
- 125000000956 methoxy group Chemical group [H]C([H])([H])O* 0.000 claims description 13
- 239000008194 pharmaceutical composition Substances 0.000 claims description 13
- 125000006714 (C3-C10) heterocyclyl group Chemical group 0.000 claims description 12
- 125000002619 bicyclic group Chemical group 0.000 claims description 12
- 125000002950 monocyclic group Chemical group 0.000 claims description 12
- 102100033793 ALK tyrosine kinase receptor Human genes 0.000 claims description 11
- 108020001507 fusion proteins Proteins 0.000 claims description 11
- 102000037865 fusion proteins Human genes 0.000 claims description 11
- 125000004432 carbon atom Chemical group C* 0.000 claims description 10
- 229910052799 carbon Inorganic materials 0.000 claims description 8
- 125000000113 cyclohexyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])(*)C([H])([H])C1([H])[H] 0.000 claims description 8
- 239000003814 drug Substances 0.000 claims description 8
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims description 8
- 125000003386 piperidinyl group Chemical group 0.000 claims description 7
- 125000004076 pyridyl group Chemical group 0.000 claims description 6
- 125000000719 pyrrolidinyl group Chemical group 0.000 claims description 6
- 125000006272 (C3-C7) cycloalkyl group Chemical group 0.000 claims description 5
- 125000001995 cyclobutyl group Chemical group [H]C1([H])C([H])([H])C([H])(*)C1([H])[H] 0.000 claims description 5
- 108700009251 p80(NPM-ALK) Proteins 0.000 claims description 5
- 125000004434 sulfur atom Chemical group 0.000 claims description 5
- 125000004196 benzothienyl group Chemical group S1C(=CC2=C1C=CC=C2)* 0.000 claims description 4
- 125000001511 cyclopentyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])(*)C1([H])[H] 0.000 claims description 4
- 125000001072 heteroaryl group Chemical group 0.000 claims description 4
- 125000001041 indolyl group Chemical group 0.000 claims description 4
- 230000002401 inhibitory effect Effects 0.000 claims description 4
- 125000002757 morpholinyl group Chemical group 0.000 claims description 4
- 239000008177 pharmaceutical agent Substances 0.000 claims description 4
- 125000004193 piperazinyl group Chemical group 0.000 claims description 4
- 125000000714 pyrimidinyl group Chemical group 0.000 claims description 4
- 125000005073 adamantyl group Chemical group C12(CC3CC(CC(C1)C3)C2)* 0.000 claims description 3
- 125000002837 carbocyclic group Chemical group 0.000 claims description 3
- 125000001559 cyclopropyl group Chemical group [H]C1([H])C([H])([H])C1([H])* 0.000 claims description 3
- 125000002393 azetidinyl group Chemical group 0.000 claims description 2
- 125000000582 cycloheptyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])([H])C([H])(*)C([H])([H])C1([H])[H] 0.000 claims description 2
- 239000003085 diluting agent Substances 0.000 claims description 2
- 125000004430 oxygen atom Chemical group O* 0.000 claims description 2
- 239000000546 pharmaceutical excipient Substances 0.000 claims description 2
- 125000000335 thiazolyl group Chemical group 0.000 claims description 2
- 125000002947 alkylene group Chemical group 0.000 claims 68
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 claims 27
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 claims 11
- 125000005869 (methoxyethoxy)methanyl group Chemical group [H]C([H])([H])OC([H])([H])C([H])([H])OC([H])([H])* 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 238000000034 method Methods 0.000 description 10
- 125000003943 azolyl group Chemical group 0.000 description 2
- 125000003373 pyrazinyl group Chemical group 0.000 description 2
- 206010006187 Breast cancer Diseases 0.000 description 1
- 208000026310 Breast neoplasm Diseases 0.000 description 1
- JGLMVXWAHNTPRF-CMDGGOBGSA-N CCN1N=C(C)C=C1C(=O)NC1=NC2=CC(=CC(OC)=C2N1C\C=C\CN1C(NC(=O)C2=CC(C)=NN2CC)=NC2=CC(=CC(OCCCN3CCOCC3)=C12)C(N)=O)C(N)=O Chemical compound CCN1N=C(C)C=C1C(=O)NC1=NC2=CC(=CC(OC)=C2N1C\C=C\CN1C(NC(=O)C2=CC(C)=NN2CC)=NC2=CC(=CC(OCCCN3CCOCC3)=C12)C(N)=O)C(N)=O JGLMVXWAHNTPRF-CMDGGOBGSA-N 0.000 description 1
- 206010009944 Colon cancer Diseases 0.000 description 1
- 208000001333 Colorectal Neoplasms Diseases 0.000 description 1
- 208000031671 Large B-Cell Diffuse Lymphoma Diseases 0.000 description 1
- 206010058467 Lung neoplasm malignant Diseases 0.000 description 1
- 206010025323 Lymphomas Diseases 0.000 description 1
- 206010027406 Mesothelioma Diseases 0.000 description 1
- 206010029260 Neuroblastoma Diseases 0.000 description 1
- 206010033128 Ovarian cancer Diseases 0.000 description 1
- 206010061535 Ovarian neoplasm Diseases 0.000 description 1
- 208000009956 adenocarcinoma Diseases 0.000 description 1
- 125000004429 atom Chemical group 0.000 description 1
- 206010012818 diffuse large B-cell lymphoma Diseases 0.000 description 1
- 230000000694 effects Effects 0.000 description 1
- 208000005017 glioblastoma Diseases 0.000 description 1
- 201000008298 histiocytosis Diseases 0.000 description 1
- 230000002757 inflammatory effect Effects 0.000 description 1
- 125000001786 isothiazolyl group Chemical group 0.000 description 1
- 201000005202 lung cancer Diseases 0.000 description 1
- 208000020816 lung neoplasm Diseases 0.000 description 1
- 210000000651 myofibroblast Anatomy 0.000 description 1
- 208000002154 non-small cell lung carcinoma Diseases 0.000 description 1
- 230000009885 systemic effect Effects 0.000 description 1
- 238000003419 tautomerization reaction Methods 0.000 description 1
- 125000004568 thiomorpholinyl group Chemical group 0.000 description 1
- 208000029729 tumor suppressor gene on chromosome 11 Diseases 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US37104110P | 2010-08-05 | 2010-08-05 | |
| US61/371,041 | 2010-08-05 | ||
| PCT/US2011/045703 WO2012018668A1 (en) | 2010-08-05 | 2011-07-28 | Benzimidazole and azabenzimidazole compounds that inhibit anaplastic lymphoma kinase |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2015159873A Division JP2016011300A (ja) | 2010-08-05 | 2015-08-13 | 未分化リンパ腫キナーゼを阻害するベンゾイミダゾール化合物およびアザベンゾイミダゾール化合物 |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2013532726A JP2013532726A (ja) | 2013-08-19 |
| JP2013532726A5 true JP2013532726A5 (enExample) | 2014-09-11 |
| JP5795635B2 JP5795635B2 (ja) | 2015-10-14 |
Family
ID=45559768
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2013523206A Expired - Fee Related JP5795635B2 (ja) | 2010-08-05 | 2011-07-28 | 未分化リンパ腫キナーゼを阻害するベンゾイミダゾール化合物およびアザベンゾイミダゾール化合物 |
| JP2015159873A Pending JP2016011300A (ja) | 2010-08-05 | 2015-08-13 | 未分化リンパ腫キナーゼを阻害するベンゾイミダゾール化合物およびアザベンゾイミダゾール化合物 |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2015159873A Pending JP2016011300A (ja) | 2010-08-05 | 2015-08-13 | 未分化リンパ腫キナーゼを阻害するベンゾイミダゾール化合物およびアザベンゾイミダゾール化合物 |
Country Status (13)
| Country | Link |
|---|---|
| US (2) | US9115127B2 (enExample) |
| EP (1) | EP2611784A4 (enExample) |
| JP (2) | JP5795635B2 (enExample) |
| KR (1) | KR20130108543A (enExample) |
| CN (1) | CN103168032A (enExample) |
| AU (2) | AU2011286005B2 (enExample) |
| BR (1) | BR112013002879A2 (enExample) |
| CA (1) | CA2807093A1 (enExample) |
| MX (1) | MX2013001313A (enExample) |
| RU (1) | RU2013109143A (enExample) |
| SG (2) | SG10201505997TA (enExample) |
| TW (1) | TWI500610B (enExample) |
| WO (1) | WO2012018668A1 (enExample) |
Families Citing this family (21)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| KR102066297B1 (ko) | 2011-10-14 | 2020-01-14 | 암비트 바이오사이언시즈 코포레이션 | 헤테로사이클릭 화합물 및 이의 유형 3 수용체 티로신 키나아제의 조절인자로서의 용도 |
| AU2012339753A1 (en) * | 2011-11-14 | 2014-06-19 | Tesaro, Inc. | Modulating certain tyrosine kinases |
| JO3300B1 (ar) | 2012-06-06 | 2018-09-16 | Novartis Ag | مركبات وتركيبات لتعديل نشاط egfr |
| US9649313B2 (en) * | 2012-11-26 | 2017-05-16 | The University Of North Carolina At Chapel Hill | Use of ITK inhibitors for the treatment of cancer |
| HK1217649A1 (zh) | 2012-12-27 | 2017-01-20 | 德雷克塞尔大学 | 針對hbv感染的新型抗病毒劑 |
| CN105829296A (zh) | 2013-12-18 | 2016-08-03 | 巴斯夫欧洲公司 | 带有亚胺衍生的取代基的唑类化合物 |
| IL291000B2 (en) | 2014-03-20 | 2024-04-01 | Capella Therapeutics Inc | Benzimidazole derivatives as erbb tyrosine kinase inhibitors for the treatment of cancer |
| CA2943231C (en) | 2014-03-20 | 2023-10-24 | Capella Therapeutics, Inc. | Benzimidazole derivatives as erbb tyrosine kinase inhibitors for the treatment of cancer |
| WO2015143652A1 (en) * | 2014-03-26 | 2015-10-01 | Merck Sharp & Dohme Corp. | TrkA KINASE INHIBITORS,COMPOSITIONS AND METHODS THEREOF |
| KR101555033B1 (ko) * | 2014-07-28 | 2015-09-23 | 충남대학교산학협력단 | 신규한 메타논 유도체, 이의 제조방법 및 이를 유효성분으로 함유하는 망막 질환의 예방 또는 치료용 약학적 조성물 |
| ES2749103T3 (es) | 2014-09-12 | 2020-03-19 | Knopp Biosciences Llc | Benzoimidazol-1,2-ilamidas como activadores del canal Kv7 |
| ES2911888T3 (es) * | 2015-09-18 | 2022-05-23 | Merck Patent Gmbh | Compuestos de heteroarilo como inhibidores de IRAK y usos de los mismos |
| KR102670695B1 (ko) | 2015-09-18 | 2024-06-05 | 메르크 파텐트 게엠베하 | Irak 억제제로서의 헤테로아릴 화합물 및 이의 용도 |
| WO2017053537A1 (en) * | 2015-09-23 | 2017-03-30 | Capella Therapeutics, Inc. | Benzimidazoles for use in the treatment of cancer and inflammatory diseases |
| CN110167938B (zh) * | 2017-01-11 | 2024-06-14 | 阿基利昂有限公司 | 作为Janus激酶抑制剂的新的氨基-咪唑并吡啶衍生物及其医药用途 |
| KR101798840B1 (ko) | 2017-05-17 | 2017-11-17 | 주식회사 레고켐 바이오사이언스 | 신규 오토탁신 저해 화합물 및 이를 함유하는 약제학적 조성물 |
| JP7313364B2 (ja) * | 2018-02-21 | 2023-07-24 | ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング | Ｅｇｆｒ阻害剤としての新たなベンズイミダゾール化合物および誘導体 |
| CN119118926A (zh) | 2018-03-19 | 2024-12-13 | 诺普生物科学有限责任公司 | Kv7通道激活剂组合物和使用方法 |
| US12522615B2 (en) | 2019-06-24 | 2026-01-13 | Boehringer Ingelheim International Gmbh | Macrocyclic compounds and derivatives as EGFR inhibitors |
| WO2021055518A1 (en) | 2019-09-17 | 2021-03-25 | University Of Utah Research Foundation | Benzimidazoles and methods of using same |
| WO2026035999A1 (en) | 2024-08-09 | 2026-02-12 | Triana Biomedicines, Inc. | Anaplastic lymphoma kinase (alk) degraders and uses thereof |
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-
2011
- 2011-07-28 SG SG10201505997TA patent/SG10201505997TA/en unknown
- 2011-07-28 RU RU2013109143/04A patent/RU2013109143A/ru not_active Application Discontinuation
- 2011-07-28 WO PCT/US2011/045703 patent/WO2012018668A1/en not_active Ceased
- 2011-07-28 JP JP2013523206A patent/JP5795635B2/ja not_active Expired - Fee Related
- 2011-07-28 BR BR112013002879A patent/BR112013002879A2/pt not_active IP Right Cessation
- 2011-07-28 CA CA2807093A patent/CA2807093A1/en not_active Abandoned
- 2011-07-28 SG SG2013006200A patent/SG187209A1/en unknown
- 2011-07-28 MX MX2013001313A patent/MX2013001313A/es not_active Application Discontinuation
- 2011-07-28 AU AU2011286005A patent/AU2011286005B2/en not_active Ceased
- 2011-07-28 CN CN2011800470711A patent/CN103168032A/zh active Pending
- 2011-07-28 EP EP11815100.0A patent/EP2611784A4/en not_active Withdrawn
- 2011-07-28 US US13/813,813 patent/US9115127B2/en active Active
- 2011-07-28 KR KR1020137005612A patent/KR20130108543A/ko not_active Withdrawn
- 2011-08-01 TW TW100127155A patent/TWI500610B/zh not_active IP Right Cessation
-
2015
- 2015-08-13 JP JP2015159873A patent/JP2016011300A/ja active Pending
- 2015-08-18 US US14/828,928 patent/US20160046625A1/en not_active Abandoned
- 2015-08-25 AU AU2015218439A patent/AU2015218439A1/en not_active Abandoned
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