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 |
| TW201107330A (en) * | 2009-07-31 | 2011-03-01 | Biocryst Pharm Inc | Heterocyclic compounds as janus kinase inhibitors |
| SG181507A1 (en) * | 2009-12-04 | 2012-07-30 | Cylene Pharmaceuticals Inc | Pyrazolopyrimidines and related heterocycles as ck2 inhibitors |
| EP2518072A4 (en) | 2009-12-24 | 2014-06-04 | Ajinomoto Kk | IMIDAZOPYRIDAZINE COMPOUNDS |
| CN102971326A (zh) * | 2010-04-28 | 2013-03-13 | 百时美施贵宝公司 | 咪唑并哒嗪化合物及其在癌症中的用途 |
| 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 |
| EP2827869A4 (en) | 2012-03-23 | 2015-09-23 | Dennis Brown | COMPOSITIONS AND METHODS FOR IMPROVING THE THERAPEUTIC BENEFIT OF INDIRUBIN AND ANALOGUE THEREOF, WITH MEISOINDIGO |
| CN104837844B (zh) * | 2012-12-21 | 2017-08-29 | 百时美施贵宝公司 | 作为酪蛋白激酶1 d/e抑制剂的吡唑取代的咪唑并哌嗪 |
| 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 |
| 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 |
| CN106661056B (zh) * | 2014-06-19 | 2019-07-05 | 百时美施贵宝公司 | 作为酪蛋白激酶1δ/ε抑制剂的咪唑并哒嗪衍生物 |
| 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 |
| 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 |
| EP3268367B8 (en) * | 2015-03-12 | 2022-11-16 | Merck Sharp & Dohme LLC | Carboxamide inhibitors of irak4 activity |
| 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 |
| 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 |
| 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 |
| 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 |
| 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 |
| 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 |
| MA45940B1 (fr) * | 2016-08-10 | 2024-12-31 | Takeda Pharmaceutical Company Limited | Composé hétérocyclique |
| 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 |
| EP3541817B1 (en) | 2016-11-17 | 2020-12-23 | Bristol-Myers Squibb Company | Imidazopyridazine modulators of il-12, il-23 and/or ifn-alpha |
| AU2018208516B2 (en) * | 2017-01-11 | 2021-07-08 | Aqilion Ab | Novel amino-imidazopyridine derivatives as Janus kinase inhibitors and pharmaceutical use thereof |
| WO2020154474A1 (en) * | 2019-01-23 | 2020-07-30 | Nimbus Lakshmi, Inc. | Tyk2 inhibitors and uses thereof |
| JP7526196B2 (ja) * | 2019-03-05 | 2024-07-31 | ブリストル－マイヤーズ スクイブ カンパニー | Ｉｌ－１２、ｉｌ－２３、および／またはｉｆｎアルファ応答の調節剤として有用なイミダゾピリダジン化合物 |
| EP4281458A4 (en) * | 2021-01-19 | 2025-01-08 | Anrui Biomedical Technology (Guangzhou) Co., Ltd. | IMIDAZOLOPYRIDAZINE OR PYRAZOLOPYRIMIDINE COMPOUNDS AND COMPOSITIONS |
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| CH635587A5 (fr) | 1978-01-09 | 1983-04-15 | Aron Sa | Derives amines de pyrazolo (1,5-a) s.triazine, therapeutiquement actifs et leurs procedes de preparation. |
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| BRPI0407834A (pt) | 2003-02-28 | 2006-02-14 | Teijin Pharma Ltd | composto, processo para a manufatura do mesmo, composição, processo para a manufatura da mesma, método de tratamento ou prevenção de um distúrbio mediado por proteìna quinase em um indivìduo, uso de um composto, ensaio para determinar a atividade dos compostos, e, método de inibição da atividade ou função de uma proteìna quinase |
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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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| BRPI0714665A2 (pt) * | 2006-08-04 | 2012-03-13 | Takeda Pharmaceutical Company Limited | Composto, pró-droga, agente farmacêutico, e, método para a profilaxia ou tratamento do câncer |
| CN101730699A (zh) | 2007-03-21 | 2010-06-09 | 百时美施贵宝公司 | 可用于治疗增殖性、变应性、自身免疫性和炎症性疾病的稠合杂环化合物 |
| US8476430B2 (en) | 2008-07-24 | 2013-07-02 | Bristol-Myers Squibb Company | Fused heterocyclic compounds useful as kinase modulators |
| 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 JP JP2010546068A patent/JP5394404B2/ja not_active Expired - Fee Related
- 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
- 2009-02-06 EP EP09709087.2A patent/EP2240488B1/en not_active Not-in-force
- 2009-02-06 WO PCT/US2009/033455 patent/WO2009100375A1/en not_active Ceased