JP2011511095A5 - - Google Patents
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- Publication number
- JP2011511095A5 JP2011511095A5 JP2010546068A JP2010546068A JP2011511095A5 JP 2011511095 A5 JP2011511095 A5 JP 2011511095A5 JP 2010546068 A JP2010546068 A JP 2010546068A JP 2010546068 A JP2010546068 A JP 2010546068A JP 2011511095 A5 JP2011511095 A5 JP 2011511095A5
- Authority
- JP
- Japan
- Prior art keywords
- substituted
- alkyl
- heterocyclo
- heteroaryl
- cycloalkyl
- 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 109
- 125000001072 heteroaryl group Chemical group 0.000 claims 68
- 125000003118 aryl group Chemical group 0.000 claims 38
- 125000003342 alkenyl group Chemical group 0.000 claims 30
- 125000000753 cycloalkyl group Chemical group 0.000 claims 28
- 229910052739 hydrogen Inorganic materials 0.000 claims 26
- 239000001257 hydrogen Substances 0.000 claims 26
- 125000000304 alkynyl group Chemical group 0.000 claims 24
- 125000003636 chemical group Chemical group 0.000 claims 23
- 125000005017 substituted alkenyl group Chemical group 0.000 claims 20
- 150000002431 hydrogen Chemical class 0.000 claims 17
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 16
- -1 pyridazinyl pyrrolidinyl Chemical group 0.000 claims 16
- 125000000547 substituted alkyl group Chemical group 0.000 claims 16
- 125000004426 substituted alkynyl group Chemical group 0.000 claims 16
- 125000003107 substituted aryl group Chemical group 0.000 claims 15
- 229910052736 halogen Inorganic materials 0.000 claims 14
- 150000002367 halogens Chemical class 0.000 claims 14
- 125000004093 cyano group Chemical group *C#N 0.000 claims 13
- 125000005346 substituted cycloalkyl group Chemical group 0.000 claims 13
- 125000006272 (C3-C7) cycloalkyl group Chemical group 0.000 claims 12
- 125000002947 alkylene group Chemical group 0.000 claims 12
- 150000001875 compounds Chemical class 0.000 claims 12
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 9
- 229910052794 bromium Inorganic materials 0.000 claims 9
- 229910052801 chlorine Inorganic materials 0.000 claims 9
- 229910052731 fluorine Inorganic materials 0.000 claims 9
- 125000004356 hydroxy functional group Chemical group O* 0.000 claims 9
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 claims 9
- 229910052757 nitrogen Inorganic materials 0.000 claims 8
- VOPWNXZWBYDODV-UHFFFAOYSA-N Chlorodifluoromethane Chemical compound FC(F)Cl VOPWNXZWBYDODV-UHFFFAOYSA-N 0.000 claims 7
- 125000004433 nitrogen atom Chemical group N* 0.000 claims 7
- 125000004076 pyridyl group Chemical group 0.000 claims 7
- 125000002950 monocyclic group Chemical group 0.000 claims 6
- 125000003226 pyrazolyl group Chemical group 0.000 claims 6
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 claims 5
- 125000001188 haloalkyl group Chemical group 0.000 claims 5
- 125000002883 imidazolyl group Chemical group 0.000 claims 5
- 125000002757 morpholinyl group Chemical group 0.000 claims 5
- 206010028980 Neoplasm Diseases 0.000 claims 3
- 125000003545 alkoxy group Chemical group 0.000 claims 3
- 201000011510 cancer Diseases 0.000 claims 3
- 125000003386 piperidinyl group Chemical group 0.000 claims 3
- 125000000714 pyrimidinyl group Chemical group 0.000 claims 3
- 125000000719 pyrrolidinyl group Chemical group 0.000 claims 3
- 125000006413 ring segment Chemical group 0.000 claims 3
- 125000000335 thiazolyl group Chemical group 0.000 claims 3
- 125000001425 triazolyl group Chemical group 0.000 claims 3
- IJGRMHOSHXDMSA-UHFFFAOYSA-N Atomic nitrogen Chemical compound N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims 2
- 125000001164 benzothiazolyl group Chemical group S1C(=NC2=C1C=CC=C2)* 0.000 claims 2
- 229910052799 carbon Inorganic materials 0.000 claims 2
- 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 2
- 239000003814 drug Substances 0.000 claims 2
- 239000003937 drug carrier Substances 0.000 claims 2
- 125000001475 halogen functional group Chemical group 0.000 claims 2
- 239000008194 pharmaceutical composition Substances 0.000 claims 2
- 125000004193 piperazinyl group Chemical group 0.000 claims 2
- 150000003839 salts Chemical class 0.000 claims 2
- 125000001424 substituent group Chemical group 0.000 claims 2
- 125000003831 tetrazolyl group Chemical group 0.000 claims 2
- 229940124597 therapeutic agent Drugs 0.000 claims 2
- 206010006187 Breast cancer Diseases 0.000 claims 1
- 208000026310 Breast neoplasm Diseases 0.000 claims 1
- 206010009944 Colon cancer Diseases 0.000 claims 1
- 206010058467 Lung neoplasm malignant Diseases 0.000 claims 1
- 208000000172 Medulloblastoma Diseases 0.000 claims 1
- 208000034578 Multiple myelomas Diseases 0.000 claims 1
- 206010029260 Neuroblastoma Diseases 0.000 claims 1
- 206010033128 Ovarian cancer Diseases 0.000 claims 1
- 206010061535 Ovarian neoplasm Diseases 0.000 claims 1
- 206010061902 Pancreatic neoplasm Diseases 0.000 claims 1
- 206010035226 Plasma cell myeloma Diseases 0.000 claims 1
- 201000004681 Psoriasis Diseases 0.000 claims 1
- 208000024770 Thyroid neoplasm Diseases 0.000 claims 1
- 230000001154 acute effect Effects 0.000 claims 1
- 125000004429 atom Chemical group 0.000 claims 1
- 210000000481 breast Anatomy 0.000 claims 1
- 239000003795 chemical substances by application Substances 0.000 claims 1
- 210000001072 colon Anatomy 0.000 claims 1
- 208000029742 colonic neoplasm Diseases 0.000 claims 1
- 239000002254 cytotoxic agent Substances 0.000 claims 1
- 229940127089 cytotoxic agent Drugs 0.000 claims 1
- 231100000599 cytotoxic agent Toxicity 0.000 claims 1
- 210000004907 gland Anatomy 0.000 claims 1
- 208000005017 glioblastoma Diseases 0.000 claims 1
- 208000032839 leukemia Diseases 0.000 claims 1
- 210000004072 lung Anatomy 0.000 claims 1
- 201000005202 lung cancer Diseases 0.000 claims 1
- 208000020816 lung neoplasm Diseases 0.000 claims 1
- 208000015486 malignant pancreatic neoplasm Diseases 0.000 claims 1
- 238000004519 manufacturing process Methods 0.000 claims 1
- 201000001441 melanoma Diseases 0.000 claims 1
- 229940127084 other anti-cancer agent Drugs 0.000 claims 1
- 230000002611 ovarian Effects 0.000 claims 1
- 201000002528 pancreatic cancer Diseases 0.000 claims 1
- 208000008443 pancreatic carcinoma Diseases 0.000 claims 1
- 210000002307 prostate Anatomy 0.000 claims 1
- 125000003373 pyrazinyl group Chemical group 0.000 claims 1
- 125000002098 pyridazinyl group Chemical group 0.000 claims 1
- JUJWROOIHBZHMG-UHFFFAOYSA-O pyridinium Chemical compound C1=CC=[NH+]C=C1 JUJWROOIHBZHMG-UHFFFAOYSA-O 0.000 claims 1
- 125000000168 pyrrolyl group Chemical group 0.000 claims 1
- 206010039073 rheumatoid arthritis Diseases 0.000 claims 1
- 125000001544 thienyl group Chemical group 0.000 claims 1
- 125000004568 thiomorpholinyl group Chemical group 0.000 claims 1
- 201000002510 thyroid cancer Diseases 0.000 claims 1
- 125000004306 triazinyl group Chemical group 0.000 claims 1
- 0 CN(*)c1c(*)c(N(*)*)n[n]2c1nc(*)c2C(N(*)*)=O Chemical compound CN(*)c1c(*)c(N(*)*)n[n]2c1nc(*)c2C(N(*)*)=O 0.000 description 2
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US2665108P | 2008-02-06 | 2008-02-06 | |
| US61/026,651 | 2008-02-06 | ||
| PCT/US2009/033455 WO2009100375A1 (en) | 2008-02-06 | 2009-02-06 | Substituted imidazopyridazines useful as kinase inhibitors |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2011511095A JP2011511095A (ja) | 2011-04-07 |
| JP2011511095A5 true JP2011511095A5 (enExample) | 2011-09-29 |
| JP5394404B2 JP5394404B2 (ja) | 2014-01-22 |
Family
ID=40566064
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2010546068A Expired - Fee Related JP5394404B2 (ja) | 2008-02-06 | 2009-02-06 | キナーゼ阻害剤として有用な置換イミダゾピリダジン類 |
Country Status (5)
| Country | Link |
|---|---|
| US (1) | US8389527B2 (enExample) |
| EP (1) | EP2240488B1 (enExample) |
| JP (1) | JP5394404B2 (enExample) |
| CN (1) | CN101981033B (enExample) |
| WO (1) | WO2009100375A1 (enExample) |
Families Citing this family (33)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| TWI491610B (zh) * | 2008-10-09 | 2015-07-11 | 必治妥美雅史谷比公司 | 作為激酶抑制劑之咪唑并嗒腈 |
| EP2210891A1 (en) * | 2009-01-26 | 2010-07-28 | Domain Therapeutics | New adenosine receptor ligands and uses thereof |
| JP2013501003A (ja) * | 2009-07-31 | 2013-01-10 | バイオクライスト ファーマシューティカルズ， インコーポレイテッド | ヤヌスキナーゼ阻害剤としてのピロロ［１，２−ｂ］ピリダジン誘導体 |
| PL2509602T3 (pl) * | 2009-12-04 | 2017-08-31 | Senhwa Biosciences, Inc. | Pirazolopirymidyny i podobne heterocykle jako inhibitory ck2 |
| EP2518072A4 (en) | 2009-12-24 | 2014-06-04 | Ajinomoto Kk | IMIDAZOPYRIDAZINE COMPOUNDS |
| WO2011137155A1 (en) * | 2010-04-28 | 2011-11-03 | Bristol-Myers Squibb Company | Imidazopyridazinyl compounds and their uses for cancer |
| TWI541243B (zh) | 2010-09-10 | 2016-07-11 | 拜耳知識產權公司 | 經取代咪唑并嗒 |
| DE102011075398A1 (de) * | 2011-05-06 | 2012-11-08 | Bayer Pharma Aktiengesellschaft | Substituierte Imidazopyridazine und ihre Verwendung |
| KR20140077963A (ko) * | 2011-10-20 | 2014-06-24 | 글락소스미스클라인 엘엘씨 | 시르투인 조절제로서의 치환된 비시클릭 아자-헤테로사이클 및 유사체 |
| WO2013142817A2 (en) | 2012-03-23 | 2013-09-26 | Dennis Brown | Compositions and methods to improve the therapeutic benefit of indirubin and analogs thereof, including meisoindigo |
| EP2935272B1 (en) * | 2012-12-21 | 2017-02-22 | Bristol-Myers Squibb Company | Pyrazole substituted imidazopyrazines as casein kinase 1 d/e inhibitors |
| TW201437211A (zh) * | 2013-03-01 | 2014-10-01 | Bayer Pharma AG | 經取代咪唑并嗒□ |
| EP3035921A1 (en) * | 2013-08-20 | 2016-06-29 | Bristol-Myers Squibb Company | Imidazopyridazine kinase inhibitors useful to treating a disease or disorder mediated by aak1, such as alzheimer's disease, bipolar disorder, pain, schizophrenia |
| CN105979950A (zh) | 2013-10-11 | 2016-09-28 | 百时美施贵宝公司 | 吡咯并三嗪激酶抑制剂 |
| ES2702126T3 (es) | 2013-12-10 | 2019-02-27 | Bristol Myers Squibb Co | Compuestos de imidazopiridazina útiles como moduladores de respuestas a IL-12, IL-23 y/o IFN alfa |
| JP6564406B2 (ja) * | 2014-06-19 | 2019-08-21 | ブリストル−マイヤーズ スクイブ カンパニーＢｒｉｓｔｏｌ−Ｍｙｅｒｓ Ｓｑｕｉｂｂ Ｃｏｍｐａｎｙ | カゼインキナーゼ１デルタ／イプシロン阻害剤としてのイミダゾ−ピリダジン誘導体 |
| EP3215511B1 (en) | 2014-11-06 | 2024-04-17 | Bial-R&D Investments, S.A. | Substituted pyrazolo(1,5-a)pyrimidines and their use in the treatment of medical disorders |
| 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 |
| WO2016073889A1 (en) | 2014-11-06 | 2016-05-12 | Lysosomal Therapeutics Inc. | Substituted imidazo[1,5-a]pyrimidines and their use in the treatment of medical disorders |
| US10155765B2 (en) * | 2015-03-12 | 2018-12-18 | Merck Sharp & Dohme Corp. | Carboxamide inhibitors of IRAK4 activity |
| KR102782807B1 (ko) * | 2015-11-18 | 2025-03-14 | 브리스톨-마이어스 스큅 컴퍼니 | Il-12, il-23 및/또는 ifn 알파 반응의 조정제로서 유용한 이미다조피리다진 화합물 |
| MX388912B (es) | 2016-04-06 | 2025-03-20 | Lysosomal Therapeutics Inc | Compuestos de pirrol[1,2-a]pirimidinil carboxamida y su uso en el tratamiento de trastornos médicos |
| KR20180133461A (ko) | 2016-04-06 | 2018-12-14 | 리소소말 테라퓨틱스 인크. | 피라졸로[1,5-a]피리미디닐 카르복스아미드 화합물 및 의학적 장애의 치료에서의 그의 용도 |
| 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 |
| 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 |
| WO2017192931A1 (en) | 2016-05-05 | 2017-11-09 | Lysosomal Therapeutics Inc. | SUBSTITUTED IMDAZO[1,2-α]PYRIDINES, SUBSTITUTED IMIDAZO[1,2-α]PYRAZINES, RELATED COMPOUNDS, AND THEIR USE IN THE TREATMENT OF MEDICAL DISORDERS |
| PL3498693T3 (pl) * | 2016-08-10 | 2025-03-24 | Takeda Pharmaceutical Company Limited | Związek heterocykliczny |
| US10836770B2 (en) | 2016-10-07 | 2020-11-17 | Bristol-Myers Squibb Company | Imidazopyridazine compounds useful as modulators of IL-12, IL-23 and/or INF alpha responses |
| US11299494B2 (en) | 2016-11-17 | 2022-04-12 | Bristol-Myers Squibb Company | Substituted imidazo[1,2-b]pyridazines as interleukin-23 and interferon-α modulators |
| 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 |
| CA3126034A1 (en) * | 2019-01-23 | 2020-07-30 | Nimbus Lakshmi, Inc. | Tyk2 inhibitors and uses thereof |
| KR102865925B1 (ko) * | 2019-03-05 | 2025-09-26 | 브리스톨-마이어스 스큅 컴퍼니 | Il-12, il-23 및/또는 ifn 알파 반응의 조정제로서 유용한 이미다조피리다진 화합물 |
| CN117043164A (zh) * | 2021-01-19 | 2023-11-10 | 安锐生物医药科技(广州)有限公司 | 咪唑并哒嗪或吡唑并嘧啶化合物和组合物 |
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| US20070078136A1 (en) * | 2005-09-22 | 2007-04-05 | Bristol-Myers Squibb Company | Fused heterocyclic compounds useful as kinase modulators |
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| TWI491610B (zh) * | 2008-10-09 | 2015-07-11 | 必治妥美雅史谷比公司 | 作為激酶抑制劑之咪唑并嗒腈 |
-
2009
- 2009-02-06 WO PCT/US2009/033455 patent/WO2009100375A1/en not_active Ceased
- 2009-02-06 JP JP2010546068A patent/JP5394404B2/ja not_active Expired - Fee Related
- 2009-02-06 EP EP09709087.2A patent/EP2240488B1/en not_active Not-in-force
- 2009-02-06 US US12/866,365 patent/US8389527B2/en active Active
- 2009-02-06 CN CN200980111092.8A patent/CN101981033B/zh not_active Expired - Fee Related