JP2015509534A5 - - Google Patents
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- Publication number
- JP2015509534A5 JP2015509534A5 JP2014561020A JP2014561020A JP2015509534A5 JP 2015509534 A5 JP2015509534 A5 JP 2015509534A5 JP 2014561020 A JP2014561020 A JP 2014561020A JP 2014561020 A JP2014561020 A JP 2014561020A JP 2015509534 A5 JP2015509534 A5 JP 2015509534A5
- Authority
- JP
- Japan
- Prior art keywords
- halo
- optionally substituted
- cyano
- pharmaceutical composition
- hydrocarbyl
- 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
- 125000005843 halogen group Chemical group 0.000 claims 43
- 125000004093 cyano group Chemical group *C#N 0.000 claims 40
- 239000008194 pharmaceutical composition Substances 0.000 claims 38
- 150000001875 compounds Chemical class 0.000 claims 35
- 125000001183 hydrocarbyl group Chemical group 0.000 claims 33
- 230000000694 effects Effects 0.000 claims 31
- 238000006467 substitution reaction Methods 0.000 claims 30
- 108091000080 Phosphotransferase Proteins 0.000 claims 29
- 102000020233 phosphotransferase Human genes 0.000 claims 29
- 239000003112 inhibitor Substances 0.000 claims 28
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 24
- 239000001257 hydrogen Substances 0.000 claims 20
- 229910052739 hydrogen Inorganic materials 0.000 claims 20
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims 14
- 150000002431 hydrogen Chemical class 0.000 claims 13
- 125000004076 pyridyl group Chemical group 0.000 claims 12
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 8
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 7
- 125000000623 heterocyclic group Chemical group 0.000 claims 7
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 7
- 125000000999 tert-butyl group Chemical group [H]C([H])([H])C(*)(C([H])([H])[H])C([H])([H])[H] 0.000 claims 7
- GLUUGHFHXGJENI-UHFFFAOYSA-N Piperazine Chemical compound C1CNCCN1 GLUUGHFHXGJENI-UHFFFAOYSA-N 0.000 claims 6
- RAXXELZNTBOGNW-UHFFFAOYSA-N imidazole Natural products C1=CNC=N1 RAXXELZNTBOGNW-UHFFFAOYSA-N 0.000 claims 6
- 150000003839 salts Chemical class 0.000 claims 6
- 125000001309 chloro group Chemical group Cl* 0.000 claims 5
- 208000002193 Pain Diseases 0.000 claims 4
- YTPLMLYBLZKORZ-UHFFFAOYSA-N Thiophene Chemical compound C=1C=CSC=1 YTPLMLYBLZKORZ-UHFFFAOYSA-N 0.000 claims 4
- 201000010099 disease Diseases 0.000 claims 4
- 208000035475 disorder Diseases 0.000 claims 4
- 208000004296 neuralgia Diseases 0.000 claims 4
- 208000021722 neuropathic pain Diseases 0.000 claims 4
- 125000003386 piperidinyl group Chemical group 0.000 claims 4
- RWRDLPDLKQPQOW-UHFFFAOYSA-N Pyrrolidine Chemical compound C1CCNC1 RWRDLPDLKQPQOW-UHFFFAOYSA-N 0.000 claims 3
- 229910052757 nitrogen Inorganic materials 0.000 claims 3
- 125000004433 nitrogen atom Chemical group N* 0.000 claims 3
- LRANPJDWHYRCER-UHFFFAOYSA-N 1,2-diazepine Chemical compound N1C=CC=CC=N1 LRANPJDWHYRCER-UHFFFAOYSA-N 0.000 claims 2
- 208000024827 Alzheimer disease Diseases 0.000 claims 2
- 208000020925 Bipolar disease Diseases 0.000 claims 2
- 208000001640 Fibromyalgia Diseases 0.000 claims 2
- 208000018737 Parkinson disease Diseases 0.000 claims 2
- 125000000217 alkyl group Chemical group 0.000 claims 2
- 125000004122 cyclic group Chemical group 0.000 claims 2
- 230000001404 mediated effect Effects 0.000 claims 2
- 230000002093 peripheral effect Effects 0.000 claims 2
- 201000000980 schizophrenia Diseases 0.000 claims 2
- 238000002560 therapeutic procedure Methods 0.000 claims 2
- 229930192474 thiophene Natural products 0.000 claims 2
- 239000003795 chemical substances by application Substances 0.000 claims 1
- 239000003085 diluting agent Substances 0.000 claims 1
- 230000005764 inhibitory process Effects 0.000 claims 1
- 238000000034 method Methods 0.000 claims 1
- 239000000546 pharmaceutical excipient Substances 0.000 claims 1
- 0 CC(C1)c2ncc(-c3cnccc3)[n]2N=C1N1C[C@@](*)CC1 Chemical compound CC(C1)c2ncc(-c3cnccc3)[n]2N=C1N1C[C@@](*)CC1 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201261608758P | 2012-03-09 | 2012-03-09 | |
| US61/608,758 | 2012-03-09 | ||
| PCT/US2013/029043 WO2013134219A1 (en) | 2012-03-09 | 2013-03-05 | Imidazo [1, 2 - b] pyridazine - based compounds, compositions comprising them, and uses thereof |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2015509534A JP2015509534A (ja) | 2015-03-30 |
| JP2015509534A5 true JP2015509534A5 (enExample) | 2016-04-14 |
| JP6418949B2 JP6418949B2 (ja) | 2018-11-07 |
Family
ID=48014284
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2014561020A Active JP6418949B2 (ja) | 2012-03-09 | 2013-03-05 | イミダゾ[1,2−b]ピリダジン系化合物、それを含む組成物、及びそれらを使用する方法 |
Country Status (19)
| Country | Link |
|---|---|
| US (3) | US8969565B2 (enExample) |
| EP (1) | EP2822559B1 (enExample) |
| JP (1) | JP6418949B2 (enExample) |
| KR (1) | KR102085121B1 (enExample) |
| CN (1) | CN104470523B (enExample) |
| AR (1) | AR090291A1 (enExample) |
| AU (1) | AU2013230119B2 (enExample) |
| BR (1) | BR112014022271B1 (enExample) |
| CA (1) | CA2866164C (enExample) |
| ES (1) | ES2676826T3 (enExample) |
| IL (1) | IL234485A (enExample) |
| MX (1) | MX347917B (enExample) |
| NZ (1) | NZ630719A (enExample) |
| RU (1) | RU2014140739A (enExample) |
| SG (1) | SG11201405563VA (enExample) |
| TW (1) | TW201341385A (enExample) |
| UY (1) | UY34669A (enExample) |
| WO (1) | WO2013134219A1 (enExample) |
| ZA (1) | ZA201406148B (enExample) |
Families Citing this family (42)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP2210891A1 (en) * | 2009-01-26 | 2010-07-28 | Domain Therapeutics | New adenosine receptor ligands and uses thereof |
| ES2834093T3 (es) | 2011-07-21 | 2021-06-16 | Sumitomo Dainippon Pharma Oncology Inc | Inhibidores de proteína quinasa heterocíclicos |
| RU2014140735A (ru) | 2012-03-09 | 2016-04-27 | Лексикон Фармасьютикалз, Инк. | ПРОИЗВОДНЫЕ ПИРАЗОЛО[1, 5-a]ПИРИМИДИНА, КОМПОЗИЦИИ, СОДЕРЖАЩИЕ УКАЗАННЫЕ СОЕДИНЕНИЯ, И СПОСОБЫ ИХ ПРИМЕНЕНИЯ |
| US8901305B2 (en) | 2012-07-31 | 2014-12-02 | Bristol-Myers Squibb Company | Aryl lactam kinase inhibitors |
| US9708337B2 (en) | 2013-02-22 | 2017-07-18 | Bristol-Myers Squibb Company | Aryl amide-based kinase inhibitors |
| AR097543A1 (es) * | 2013-09-06 | 2016-03-23 | Lexicon Pharmaceuticals Inc | COMPUESTOS BASADOS EN IMIDAZO[1,2-b]PIRIDAZINA, COMPOSICIONES QUE LOS COMPRENDEN Y SUS MÉTODOS DE USO |
| ES2678877T3 (es) | 2013-10-11 | 2018-08-20 | Bristol-Myers Squibb Company | Inhibidores de pirrolotriazina quinasa |
| CN105992768B (zh) * | 2013-12-10 | 2018-04-20 | 百时美施贵宝公司 | 用作IL‑12、IL‑23和/或IFNα响应的调节剂的咪唑并哒嗪化合物 |
| PL3097107T3 (pl) * | 2014-01-24 | 2020-01-31 | Turning Point Therapeutics, Inc. | Diarylowe związki makrocykliczne jako modulatory kinaz białkowych |
| MX2016009352A (es) * | 2014-01-31 | 2016-10-13 | Bristol Myers Squibb Co | Inhibidores de quinasa a base de quinolina. |
| TW201620911A (zh) * | 2014-03-17 | 2016-06-16 | 雷西肯製藥股份有限公司 | 銜接子關聯激酶1之抑制劑、包含其之組成物、及其使用方法 |
| US20170239249A1 (en) * | 2014-09-30 | 2017-08-24 | Bristol-Myers Squibb Company | Quinazoline-based kinase inhibitors |
| US20170333435A1 (en) | 2014-11-06 | 2017-11-23 | Lysosomal Therapeutics Inc. | Substituted imidazo[1,5-a]pyrimidines and their use in the treatment of medical disorders |
| KR102662215B1 (ko) | 2014-11-06 | 2024-05-02 | 비알 - 알&디 인베스트먼츠, 에스.에이. | 치환된 피라졸로(1,5-a)피리미딘 및 의학적 장애의 치료에서의 그의 용도 |
| WO2016073891A1 (en) | 2014-11-06 | 2016-05-12 | Lysosomal Therapeutics Inc. | Substituted pyrrolo[1,2-a]pyrimidines and their use in the treatment of medical disorders |
| WO2016164295A2 (en) | 2015-04-10 | 2016-10-13 | Bristol-Myers Squibb Company | Fused pyridines as kinase inhibitors |
| AU2016287568B2 (en) | 2015-07-02 | 2020-08-20 | Turning Point Therapeutics, Inc. | Chiral diaryl macrocycles as modulators of protein kinases |
| HRP20240780T1 (hr) * | 2015-07-06 | 2024-09-13 | Turning Point Therapeutics, Inc. | Polimorf diaril makrocikla |
| KR102772574B1 (ko) | 2015-07-21 | 2025-02-24 | 터닝 포인트 테라퓨틱스, 인크. | 키랄 디아릴 매크로사이클 및 이것의 용도 |
| US10479793B2 (en) | 2015-11-18 | 2019-11-19 | Bristol-Myers Squibb Company | Imidazopyridazine compounds useful as modulators of IL-12, IL-23 and/or IFN alpha responses |
| US11192892B2 (en) | 2016-04-06 | 2021-12-07 | Bial—R&D Investments, S.A. | Substituted pyrazolo[1,5-a]pyrimidines for the treatment of medical disorders |
| JP7034935B2 (ja) | 2016-04-06 | 2022-03-14 | リソソーマル・セラピューティクス・インコーポレイテッド | ピロロ[1,2-a]ピリミジニルカルボキサミド化合物および医学的障害の処置におけるその使用 |
| WO2017176961A1 (en) | 2016-04-06 | 2017-10-12 | Lysosomal Therapeutics Inc. | Imidazo [1,5-a]pyrimidinyl carboxamide compounds and their use in the treatment of medical disorders |
| FI3442977T3 (fi) * | 2016-04-15 | 2023-09-26 | Blueprint Medicines Corp | Aktiviinireseptorin kaltaisen kinaasin estäjät |
| US11345698B2 (en) | 2016-05-05 | 2022-05-31 | Bial—R&D Investments, S.A. | Substituted imidazo[1,2-a]pyridines, substituted imidazo[1,2-a]pyrazines, related compounds, and their use in the treatment of medical disorders |
| WO2017192930A1 (en) | 2016-05-05 | 2017-11-09 | Lysosomal Therapeutics Inc. | SUBSTITUTED IMIDAZO[1,2-b]PYRIDAZINES, SUBSTITUTED IMIDAZO[1,5-b]PYRIDAZINES, RELATED COMPOUNDS, AND THEIR USE IN THE TREATMENT OF MEDICAL DISORDERS |
| RU2019105587A (ru) | 2016-07-28 | 2020-08-28 | Тёрнинг Поинт Терапьютикс, Инк. | Макроциклические ингибиторы киназ |
| GB201617758D0 (en) | 2016-10-20 | 2016-12-07 | Almac Discovery Limited | Pharmaceutical compounds |
| TWI808958B (zh) | 2017-01-25 | 2023-07-21 | 美商特普醫葯公司 | 涉及二芳基巨環化合物之組合療法 |
| KR102719387B1 (ko) * | 2017-01-26 | 2024-10-21 | 한미약품 주식회사 | 이미다조피리다진 화합물 |
| CN114773351A (zh) * | 2017-03-14 | 2022-07-22 | 第一三共株式会社 | 制备3,6-二取代咪唑并[1,2-b]哒嗪衍生物的方法 |
| CN107082828B (zh) * | 2017-05-19 | 2019-09-17 | 暨南大学 | 一种活性氧响应性高分子载体及其制备方法 |
| JP7224334B2 (ja) | 2017-07-28 | 2023-02-17 | ターニング・ポイント・セラピューティクス・インコーポレイテッド | 大環式化合物およびその使用 |
| US10899733B2 (en) | 2017-08-23 | 2021-01-26 | Oregon Health & Science University | Inhibitors of PARPs that catalyze mono-ADP-ribosylation |
| SI3728271T1 (sl) | 2017-12-19 | 2023-01-31 | Turning Point Therapeutics, Inc. | Makrociklične spojine za zdravljenje bolezni |
| HUE072069T2 (hu) | 2019-02-12 | 2025-10-28 | Sumitomo Pharma America Inc | 2-((1R,4R)-4-((3-(3-(trifluormetil)fenil)imidazo[1,2- b]piridazin-6-il)amino)ciklohexil)propán-2-ol sósavas sójának kristályos formája |
| CN110684028B (zh) * | 2019-10-28 | 2021-10-26 | 上海阿拉丁生化科技股份有限公司 | 一种2,6-二氮杂双环[3,3,0]辛烷类化合物的制备方法 |
| US12435091B2 (en) | 2020-04-21 | 2025-10-07 | The Uab Research Foundation | RNA-binding protein multimerization inhibitors and methods of use thereof |
| KR102590438B1 (ko) * | 2020-10-16 | 2023-10-18 | 김홍렬 | Pmca 억제제를 포함하는 코로나바이러스 감염 또는 감염 질환의 예방 또는 소독용 조성물 |
| KR102590444B1 (ko) * | 2020-10-16 | 2023-10-18 | 김홍렬 | Pmca 억제제를 포함하는 코로나바이러스 감염 또는 감염 질환의 치료용 조성물 |
| CN117120090A (zh) * | 2021-02-12 | 2023-11-24 | 林伯士萨顿公司 | Hpk1拮抗剂和其用途 |
| EP4313989A4 (en) | 2021-03-29 | 2025-03-05 | Nimbus Saturn, Inc. | HPK1 ANTAGONISTS AND USES THEREOF |
Family Cites Families (11)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US5464764A (en) | 1989-08-22 | 1995-11-07 | University Of Utah Research Foundation | Positive-negative selection methods and vectors |
| AU2515992A (en) | 1991-08-20 | 1993-03-16 | Genpharm International, Inc. | Gene targeting in animal cells using isogenic dna constructs |
| WO2007025090A2 (en) | 2005-08-25 | 2007-03-01 | Kalypsys, Inc. | Heterobicyclic and - tricyclic inhibitors of mapk/erk kinase |
| US7750000B2 (en) * | 2005-09-02 | 2010-07-06 | Bayer Schering Pharma Ag | Substituted imidazo[1,2b]pyridazines as kinase inhibitors, their preparation and use as medicaments |
| US20070078136A1 (en) | 2005-09-22 | 2007-04-05 | Bristol-Myers Squibb Company | Fused heterocyclic compounds useful as kinase modulators |
| JP2010502716A (ja) * | 2006-09-07 | 2010-01-28 | バイオジェン・アイデック・エムエイ・インコーポレイテッド | インターロイキン1受容体関連キナーゼの調節物質 |
| CA2667962A1 (en) * | 2006-10-30 | 2008-05-08 | Novartis Ag | Heterocyclic compounds as antiinflammatory agents |
| FR2934994B1 (fr) * | 2008-08-12 | 2010-09-17 | Sanofi Aventis | Derives de 2-alkyl-6cycloamino-3-(pyridin-4-yl)imidaz°1,2-b! pyridazine, leur preparation et leur application en therapeutique |
| ES2464461T3 (es) * | 2008-09-22 | 2014-06-02 | Array Biopharma, Inc. | Compuestos de imidazo[1,2B]piridazina sustituidos como inhibidores de la TRK cinasa |
| RU2014140735A (ru) | 2012-03-09 | 2016-04-27 | Лексикон Фармасьютикалз, Инк. | ПРОИЗВОДНЫЕ ПИРАЗОЛО[1, 5-a]ПИРИМИДИНА, КОМПОЗИЦИИ, СОДЕРЖАЩИЕ УКАЗАННЫЕ СОЕДИНЕНИЯ, И СПОСОБЫ ИХ ПРИМЕНЕНИЯ |
| HUE036040T2 (hu) * | 2012-03-09 | 2018-06-28 | Lexicon Pharmaceuticals Inc | Adaptor-asszociált kináz 1 gátlása fájdalom kezelésére |
-
2013
- 2013-03-05 KR KR1020147028073A patent/KR102085121B1/ko active Active
- 2013-03-05 AU AU2013230119A patent/AU2013230119B2/en active Active
- 2013-03-05 BR BR112014022271-1A patent/BR112014022271B1/pt active IP Right Grant
- 2013-03-05 MX MX2014010584A patent/MX347917B/es active IP Right Grant
- 2013-03-05 SG SG11201405563VA patent/SG11201405563VA/en unknown
- 2013-03-05 US US13/785,271 patent/US8969565B2/en active Active
- 2013-03-05 EP EP13712953.2A patent/EP2822559B1/en active Active
- 2013-03-05 ES ES13712953.2T patent/ES2676826T3/es active Active
- 2013-03-05 JP JP2014561020A patent/JP6418949B2/ja active Active
- 2013-03-05 NZ NZ630719A patent/NZ630719A/en unknown
- 2013-03-05 WO PCT/US2013/029043 patent/WO2013134219A1/en not_active Ceased
- 2013-03-05 CN CN201380021272.3A patent/CN104470523B/zh active Active
- 2013-03-05 RU RU2014140739A patent/RU2014140739A/ru not_active Application Discontinuation
- 2013-03-05 CA CA2866164A patent/CA2866164C/en active Active
- 2013-03-08 TW TW102108279A patent/TW201341385A/zh unknown
- 2013-03-11 UY UY0001034669A patent/UY34669A/es not_active Application Discontinuation
- 2013-03-11 AR ARP130100764A patent/AR090291A1/es unknown
-
2014
- 2014-08-21 ZA ZA2014/06148A patent/ZA201406148B/en unknown
- 2014-09-07 IL IL234485A patent/IL234485A/en active IP Right Grant
-
2015
- 2015-02-25 US US14/631,097 patent/US20160024093A1/en not_active Abandoned
-
2016
- 2016-04-26 US US15/138,460 patent/US20170057964A1/en not_active Abandoned