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 (OSRAM) | 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 (OSRAM) |
| EP (1) | EP2822559B1 (OSRAM) |
| JP (1) | JP6418949B2 (OSRAM) |
| KR (1) | KR102085121B1 (OSRAM) |
| CN (1) | CN104470523B (OSRAM) |
| AR (1) | AR090291A1 (OSRAM) |
| AU (1) | AU2013230119B2 (OSRAM) |
| BR (1) | BR112014022271B1 (OSRAM) |
| CA (1) | CA2866164C (OSRAM) |
| ES (1) | ES2676826T3 (OSRAM) |
| IL (1) | IL234485A (OSRAM) |
| MX (1) | MX347917B (OSRAM) |
| NZ (1) | NZ630719A (OSRAM) |
| RU (1) | RU2014140739A (OSRAM) |
| SG (1) | SG11201405563VA (OSRAM) |
| TW (1) | TW201341385A (OSRAM) |
| UY (1) | UY34669A (OSRAM) |
| WO (1) | WO2013134219A1 (OSRAM) |
| ZA (1) | ZA201406148B (OSRAM) |
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 |
| US9416132B2 (en) | 2011-07-21 | 2016-08-16 | Tolero Pharmaceuticals, Inc. | Substituted imidazo[1,2-b]pyridazines as protein kinase inhibitors |
| PL2834243T3 (pl) | 2012-03-09 | 2018-09-28 | Lexicon Pharmaceuticals, Inc. | Związki na bazie pirazolo[1,5-a]pirymidyny, zawierające je kompozycje i sposoby ich zastosowania |
| US8901305B2 (en) | 2012-07-31 | 2014-12-02 | Bristol-Myers Squibb Company | Aryl lactam kinase inhibitors |
| JP2016509066A (ja) | 2013-02-22 | 2016-03-24 | ブリストル−マイヤーズ スクイブ カンパニーＢｒｉｓｔｏｌ−Ｍｙｅｒｓ Ｓｑｕｉｂｂ Ｃｏｍｐａｎｙ | アダプター関連キナーゼ１（ａａｋ１）の阻害剤としての５ｈ−クロメノ［３，４−ｃ］ピリジン |
| 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 |
| EP3080131B1 (en) * | 2013-12-10 | 2018-10-10 | Bristol-Myers Squibb Company | Imidazopyridazine compounds useful as modulators of il-12, il-23 and/or ifn alpha responses |
| EP3636649B1 (en) | 2014-01-24 | 2024-02-14 | Turning Point Therapeutics, Inc. | Diaryl macrocycles as modulators of protein kinases |
| ES2701903T3 (es) * | 2014-01-31 | 2019-02-26 | Bristol Myers Squibb Co | Inhibidores de cinasa 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 |
| EP3200797A1 (en) * | 2014-09-30 | 2017-08-09 | Bristol-Myers Squibb Company | Quinazoline-based kinase inhibitors |
| US20180185368A1 (en) | 2014-11-06 | 2018-07-05 | Lysosomal Therapeutics Inc. | Substituted pyrrolo[1,2-a]pyrimidines and their use in the treatment of medical disorders |
| ES2958391T3 (es) | 2014-11-06 | 2024-02-08 | Bial R&D Invest S A | Imidazo[1,5-a]pirimidinas sustituidas y su uso en el tratamiento de trastornos médicos |
| 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 |
| EP3292124B1 (en) | 2015-04-10 | 2019-05-22 | Bristol-Myers Squibb Company | 6h-isochromeno[3,4-c]pyridines and benzo[c][1,7]naphthyridin-6-(5h)-ones as adaptor associated kinase 1 (aak1) inhibitors |
| RU2732405C2 (ru) | 2015-07-02 | 2020-09-16 | Тёрнинг Поинт Терапьютикс, Инк. | Хиральные диарильные макроциклы в качестве модуляторов протеинкиназ |
| WO2017007759A1 (en) * | 2015-07-06 | 2017-01-12 | Tp Therapeutics, Inc. | Diaryl macrocycle polymorph |
| US20180325901A1 (en) | 2015-07-21 | 2018-11-15 | Tp Therapeutics, Inc. | Chiral diaryl macrocycles and uses thereof |
| 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 |
| US10787454B2 (en) | 2016-04-06 | 2020-09-29 | BIAL—BioTech Investments, Inc. | Imidazo[1,5-a]pyrimidinyl carboxamide compounds and their use in the treatment of medical disorders |
| KR20230104752A9 (ko) | 2016-04-06 | 2024-11-15 | 비알 - 알&디 인베스트먼츠, 에스.에이. | 피라졸로[1,5-a]피리미디닐 카르복스아미드 화합물및 의학적 장애의 치료에서의 그의 용도 |
| CA3020310A1 (en) | 2016-04-06 | 2017-10-12 | Lysosomal Therapeutics Inc. | Pyrrolo[1,2-a]pyrimidinyl carboxamide compounds and their use in the treatment of medical disorders |
| EP3442977B1 (en) * | 2016-04-15 | 2023-06-28 | Blueprint Medicines Corporation | Inhibitors of activin receptor-like kinase |
| EP3452455A4 (en) | 2016-05-05 | 2019-11-13 | Lysosomal Therapeutics Inc. | SUBSTITUTED IMDAZO [1,2-] PYRIDINES, SUBSTITUTED IMIDAZO [1,2-] PYRAZINES, RELATED COMPOUNDS AND THEIR USE IN THE TREATMENT OF ILLNESSES |
| JP7164774B2 (ja) | 2016-05-05 | 2022-11-02 | ビアル－アール・アンド・ディ・インベストメンツ・ソシエダーデ・アノニマ | 置換イミダゾ［１，２－ｂ］ピリダジン、置換イミダゾ［１，５－ｂ］ピリダジン、関連化合物、および医学的障害の治療におけるその使用 |
| JP2019527230A (ja) | 2016-07-28 | 2019-09-26 | 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Ｔｕｒｎｉｎｇ Ｐｏｉｎｔ Ｔｈｅｒａｐｅｕｔｉｃｓ，Ｉｎｃ． | 大環状キナーゼ阻害剤 |
| 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 |
| JP7082608B2 (ja) | 2017-03-14 | 2022-06-08 | 第一三共株式会社 | ３，６－ジ置換イミダゾ［１，２－ｂ］ピリダジン誘導体の製造方法 |
| 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 |
| LT3658148T (lt) | 2017-07-28 | 2024-09-10 | Turning Point Therapeutics, Inc. | Makrocikliniai junginiai ir jų panaudojimas |
| US10899733B2 (en) | 2017-08-23 | 2021-01-26 | Oregon Health & Science University | Inhibitors of PARPs that catalyze mono-ADP-ribosylation |
| KR102814342B1 (ko) | 2017-12-19 | 2025-05-29 | 터닝 포인트 테라퓨틱스, 인크. | 질병 치료용 대환식 화합물 |
| CA3127502A1 (en) | 2019-02-12 | 2020-08-20 | Sumitomo Dainippon Pharma Oncology, Inc. | Formulations comprising heterocyclic protein kinase inhibitors |
| 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 |
| KR102590444B1 (ko) * | 2020-10-16 | 2023-10-18 | 김홍렬 | Pmca 억제제를 포함하는 코로나바이러스 감염 또는 감염 질환의 치료용 조성물 |
| KR102590438B1 (ko) * | 2020-10-16 | 2023-10-18 | 김홍렬 | Pmca 억제제를 포함하는 코로나바이러스 감염 또는 감염 질환의 예방 또는 소독용 조성물 |
| US12252488B2 (en) * | 2021-02-12 | 2025-03-18 | Nimbus Saturn, Inc. | HPK1 antagonists and uses thereof |
| US12071442B2 (en) | 2021-03-29 | 2024-08-27 | Nimbus Saturn, Inc. | Substituted pyrrolo[3,4-c]pyridines as HPK1 antagonists |
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 |
| WO1993004169A1 (en) | 1991-08-20 | 1993-03-04 | 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 |
| US20110021513A1 (en) | 2006-09-07 | 2011-01-27 | Biogen Idec Ma Inc. | Modulators of interleukin-1 receptor-associated kinase |
| 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 |
| SI2350075T1 (sl) * | 2008-09-22 | 2014-06-30 | Array Biopharma, Inc. | Substituirane imidazo (1,2b)piridazinske spojine kot Trk kinazni inhibitorji |
| HUE036040T2 (hu) * | 2012-03-09 | 2018-06-28 | Lexicon Pharmaceuticals Inc | Adaptor-asszociált kináz 1 gátlása fájdalom kezelésére |
| PL2834243T3 (pl) | 2012-03-09 | 2018-09-28 | Lexicon Pharmaceuticals, Inc. | Związki na bazie pirazolo[1,5-a]pirymidyny, zawierające je kompozycje i sposoby ich zastosowania |
-
2013
- 2013-03-05 WO PCT/US2013/029043 patent/WO2013134219A1/en not_active Ceased
- 2013-03-05 ES ES13712953.2T patent/ES2676826T3/es active Active
- 2013-03-05 KR KR1020147028073A patent/KR102085121B1/ko active Active
- 2013-03-05 MX MX2014010584A patent/MX347917B/es active IP Right Grant
- 2013-03-05 JP JP2014561020A patent/JP6418949B2/ja active Active
- 2013-03-05 AU AU2013230119A patent/AU2013230119B2/en active Active
- 2013-03-05 US US13/785,271 patent/US8969565B2/en active Active
- 2013-03-05 CN CN201380021272.3A patent/CN104470523B/zh active Active
- 2013-03-05 NZ NZ630719A patent/NZ630719A/en unknown
- 2013-03-05 EP EP13712953.2A patent/EP2822559B1/en active Active
- 2013-03-05 RU RU2014140739A patent/RU2014140739A/ru not_active Application Discontinuation
- 2013-03-05 SG SG11201405563VA patent/SG11201405563VA/en unknown
- 2013-03-05 CA CA2866164A patent/CA2866164C/en active Active
- 2013-03-05 BR BR112014022271-1A patent/BR112014022271B1/pt active IP Right Grant
- 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
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