JP2010524957A5 - - Google Patents
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- Publication number
- JP2010524957A5 JP2010524957A5 JP2010504237A JP2010504237A JP2010524957A5 JP 2010524957 A5 JP2010524957 A5 JP 2010524957A5 JP 2010504237 A JP2010504237 A JP 2010504237A JP 2010504237 A JP2010504237 A JP 2010504237A JP 2010524957 A5 JP2010524957 A5 JP 2010524957A5
- Authority
- JP
- Japan
- Prior art keywords
- substituted
- alkyl
- aryl
- heteroaryl
- heterocyclyl
- 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
- 125000001072 heteroaryl group Chemical group 0.000 claims 71
- 125000000623 heterocyclic group Chemical group 0.000 claims 59
- -1 amino, substituted Amino Chemical group 0.000 claims 56
- 125000000547 substituted alkyl group Chemical group 0.000 claims 38
- 125000000217 alkyl group Chemical group 0.000 claims 32
- 125000000592 heterocycloalkyl group Chemical group 0.000 claims 32
- 125000003107 substituted aryl group Chemical group 0.000 claims 32
- 125000003118 aryl group Chemical group 0.000 claims 28
- 125000001589 carboacyl group Chemical group 0.000 claims 28
- 125000000392 cycloalkenyl group Chemical group 0.000 claims 28
- 125000004390 alkyl sulfonyl group Chemical group 0.000 claims 26
- 125000003282 alkyl amino group Chemical group 0.000 claims 24
- 125000004103 aminoalkyl group Chemical group 0.000 claims 24
- 125000004404 heteroalkyl group Chemical group 0.000 claims 24
- 229910052739 hydrogen Inorganic materials 0.000 claims 24
- 239000001257 hydrogen Substances 0.000 claims 24
- 125000004435 hydrogen atom Chemical class [H]* 0.000 claims 24
- 125000000753 cycloalkyl group Chemical group 0.000 claims 22
- 229910052736 halogen Inorganic materials 0.000 claims 22
- 150000002367 halogens Chemical class 0.000 claims 22
- 125000005346 substituted cycloalkyl group Chemical group 0.000 claims 22
- 150000001408 amides Chemical class 0.000 claims 18
- 125000003917 carbamoyl group Chemical group [H]N([H])C(*)=O 0.000 claims 16
- 125000004043 oxo group Chemical group O=* 0.000 claims 16
- KXDHJXZQYSOELW-UHFFFAOYSA-M Carbamate Chemical class NC([O-])=O KXDHJXZQYSOELW-UHFFFAOYSA-M 0.000 claims 14
- 125000003342 alkenyl group Chemical group 0.000 claims 14
- 125000004453 alkoxycarbonyl group Chemical group 0.000 claims 14
- 125000004644 alkyl sulfinyl group Chemical group 0.000 claims 14
- 125000000304 alkynyl group Chemical group 0.000 claims 14
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 claims 14
- 125000001188 haloalkyl group Chemical group 0.000 claims 14
- 125000005017 substituted alkenyl group Chemical group 0.000 claims 14
- 125000004426 substituted alkynyl group Chemical group 0.000 claims 14
- 125000003545 alkoxy group Chemical group 0.000 claims 12
- 125000004457 alkyl amino carbonyl group Chemical group 0.000 claims 12
- 125000004448 alkyl carbonyl group Chemical group 0.000 claims 12
- 125000005196 alkyl carbonyloxy group Chemical group 0.000 claims 12
- 125000004414 alkyl thio group Chemical group 0.000 claims 12
- 125000001118 alkylidene group Chemical group 0.000 claims 12
- 125000005140 aralkylsulfonyl group Chemical group 0.000 claims 12
- 125000005098 aryl alkoxy carbonyl group Chemical group 0.000 claims 12
- 125000003710 aryl alkyl group Chemical group 0.000 claims 12
- 125000005160 aryl oxy alkyl group Chemical group 0.000 claims 12
- 125000004391 aryl sulfonyl group Chemical group 0.000 claims 12
- 125000005325 aryloxy aryl group Chemical group 0.000 claims 12
- 150000004657 carbamic acid derivatives Chemical class 0.000 claims 12
- 125000001316 cycloalkyl alkyl group Chemical group 0.000 claims 12
- 125000004438 haloalkoxy group Chemical group 0.000 claims 12
- 125000004446 heteroarylalkyl group Chemical group 0.000 claims 12
- 125000004356 hydroxy functional group Chemical group O* 0.000 claims 12
- 125000002768 hydroxyalkyl group Chemical group 0.000 claims 12
- 150000001875 compounds Chemical class 0.000 claims 11
- OAKJQQAXSVQMHS-UHFFFAOYSA-N Hydrazine Chemical class NN OAKJQQAXSVQMHS-UHFFFAOYSA-N 0.000 claims 10
- 125000004423 acyloxy group Chemical group 0.000 claims 10
- 125000005236 alkanoylamino group Chemical group 0.000 claims 10
- 125000001691 aryl alkyl amino group Chemical group 0.000 claims 10
- 125000004659 aryl alkyl thio group Chemical group 0.000 claims 10
- 125000002102 aryl alkyloxo group Chemical group 0.000 claims 10
- 125000001769 aryl amino group Chemical group 0.000 claims 10
- 125000005110 aryl thio group Chemical group 0.000 claims 10
- 125000004104 aryloxy group Chemical group 0.000 claims 10
- 125000005112 cycloalkylalkoxy group Chemical group 0.000 claims 10
- 125000005114 heteroarylalkoxy group Chemical group 0.000 claims 10
- 125000005553 heteroaryloxy group Chemical group 0.000 claims 10
- 150000003839 salts Chemical class 0.000 claims 10
- 125000004001 thioalkyl group Chemical group 0.000 claims 8
- 241001024304 Mino Species 0.000 claims 6
- 206010028980 Neoplasm Diseases 0.000 claims 6
- 125000005239 aroylamino group Chemical group 0.000 claims 6
- 125000005129 aryl carbonyl group Chemical group 0.000 claims 6
- 201000011510 cancer Diseases 0.000 claims 6
- RAXXELZNTBOGNW-UHFFFAOYSA-N imidazole Chemical group C1=CNC=N1 RAXXELZNTBOGNW-UHFFFAOYSA-N 0.000 claims 6
- 241001553014 Myrsine salicina Species 0.000 claims 4
- 125000004658 aryl carbonyl amino group Chemical group 0.000 claims 4
- 125000000446 sulfanediyl group Chemical group *S* 0.000 claims 4
- 239000013543 active substance Substances 0.000 claims 3
- 229940127084 other anti-cancer agent Drugs 0.000 claims 3
- 206010006187 Breast cancer Diseases 0.000 claims 2
- 208000026310 Breast neoplasm Diseases 0.000 claims 2
- 206010009944 Colon cancer Diseases 0.000 claims 2
- 206010058467 Lung neoplasm malignant Diseases 0.000 claims 2
- 208000000172 Medulloblastoma Diseases 0.000 claims 2
- 208000034578 Multiple myelomas Diseases 0.000 claims 2
- 206010029260 Neuroblastoma Diseases 0.000 claims 2
- 206010033128 Ovarian cancer Diseases 0.000 claims 2
- 206010061535 Ovarian neoplasm Diseases 0.000 claims 2
- 206010061902 Pancreatic neoplasm Diseases 0.000 claims 2
- 206010035226 Plasma cell myeloma Diseases 0.000 claims 2
- 206010060862 Prostate cancer Diseases 0.000 claims 2
- 208000000236 Prostatic Neoplasms Diseases 0.000 claims 2
- 208000024770 Thyroid neoplasm Diseases 0.000 claims 2
- 230000001154 acute effect Effects 0.000 claims 2
- 210000001185 bone marrow Anatomy 0.000 claims 2
- 125000002915 carbonyl group Chemical group [*:2]C([*:1])=O 0.000 claims 2
- 208000029742 colonic neoplasm Diseases 0.000 claims 2
- 239000002254 cytotoxic agent Substances 0.000 claims 2
- 231100000599 cytotoxic agent Toxicity 0.000 claims 2
- 229940127089 cytotoxic agent Drugs 0.000 claims 2
- 239000003814 drug Substances 0.000 claims 2
- 239000003937 drug carrier Substances 0.000 claims 2
- 208000005017 glioblastoma Diseases 0.000 claims 2
- 208000032839 leukemia Diseases 0.000 claims 2
- 201000005202 lung cancer Diseases 0.000 claims 2
- 208000020816 lung neoplasm Diseases 0.000 claims 2
- 208000015486 malignant pancreatic neoplasm Diseases 0.000 claims 2
- 201000001441 melanoma Diseases 0.000 claims 2
- 201000002528 pancreatic cancer Diseases 0.000 claims 2
- 208000008443 pancreatic carcinoma Diseases 0.000 claims 2
- 201000008129 pancreatic ductal adenocarcinoma Diseases 0.000 claims 2
- 239000008194 pharmaceutical composition Substances 0.000 claims 2
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims 2
- 125000003226 pyrazolyl group Chemical group 0.000 claims 2
- 230000001568 sexual effect Effects 0.000 claims 2
- 125000005415 substituted alkoxy group Chemical group 0.000 claims 2
- OJXASOYYODXRPT-UHFFFAOYSA-N sulfamoylurea Chemical class NC(=O)NS(N)(=O)=O OJXASOYYODXRPT-UHFFFAOYSA-N 0.000 claims 2
- 229940124530 sulfonamide Drugs 0.000 claims 2
- 150000003456 sulfonamides Chemical class 0.000 claims 2
- 201000002510 thyroid cancer Diseases 0.000 claims 2
- 208000024827 Alzheimer disease Diseases 0.000 claims 1
- 241000124008 Mammalia Species 0.000 claims 1
- 239000013066 combination product Substances 0.000 claims 1
- 229940127555 combination product Drugs 0.000 claims 1
- 238000004519 manufacturing process Methods 0.000 claims 1
- 229940124597 therapeutic agent Drugs 0.000 claims 1
- 238000002560 therapeutic procedure Methods 0.000 claims 1
- 231100000167 toxic agent Toxicity 0.000 claims 1
- 239000003440 toxic substance Substances 0.000 claims 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US91244607P | 2007-04-18 | 2007-04-18 | |
| US60/912,446 | 2007-04-18 | ||
| PCT/US2008/060551 WO2008131050A1 (en) | 2007-04-18 | 2008-04-17 | Pyrrolotriazine kinase inhibitors |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2010524957A JP2010524957A (ja) | 2010-07-22 |
| JP2010524957A5 true JP2010524957A5 (enExample) | 2011-04-28 |
| JP5319659B2 JP5319659B2 (ja) | 2013-10-16 |
Family
ID=39544952
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2010504237A Expired - Fee Related JP5319659B2 (ja) | 2007-04-18 | 2008-04-17 | ピロロトリアジンキナーゼ阻害剤 |
Country Status (5)
| Country | Link |
|---|---|
| US (1) | US8198438B2 (enExample) |
| EP (1) | EP2134716A1 (enExample) |
| JP (1) | JP5319659B2 (enExample) |
| CN (1) | CN101687874B (enExample) |
| WO (1) | WO2008131050A1 (enExample) |
Families Citing this family (21)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US8268998B2 (en) | 2006-11-03 | 2012-09-18 | Bristol-Myers Squibb Company | Pyrrolotriazine kinase inhibitors |
| CN101535312B (zh) | 2006-11-03 | 2013-04-24 | 百时美施贵宝公司 | 吡咯并三嗪激酶抑制剂 |
| EP2145021A2 (en) | 2007-05-17 | 2010-01-20 | Bristol-Myers Squibb Company | Biomarkers and methods for determining sensitivity to insulin growth factor-1 receptor modulators |
| CN102015719A (zh) | 2008-03-06 | 2011-04-13 | 百时美施贵宝公司 | 吡咯并三嗪激酶抑制剂 |
| US20110269740A1 (en) * | 2008-07-02 | 2011-11-03 | Ambit Biosciences Corporation | Jak kinase modulating compounds and methods of use thereof |
| EP2344504B1 (en) * | 2008-10-08 | 2014-06-04 | Bristol-Myers Squibb Company | Pyrrolotriazine kinase inhibitors |
| WO2011089400A1 (en) | 2010-01-22 | 2011-07-28 | Centro Nacional De Investigaciones Oncológicas (Cnio) | Inhibitors of pi3 kinase |
| JP5752232B2 (ja) | 2010-03-31 | 2015-07-22 | ブリストル−マイヤーズ スクイブ カンパニーＢｒｉｓｔｏｌ−Ｍｙｅｒｓ Ｓｑｕｉｂｂ Ｃｏｍｐａｎｙ | プロテインキナーゼ阻害剤としての置換ピロロトリアジン化合物 |
| WO2011141713A1 (en) | 2010-05-13 | 2011-11-17 | Centro Nacional De Investigaciones Oncologicas (Cnio) | New bicyclic compounds as pi3-k and mtor inhibitors |
| JP6097820B2 (ja) * | 2012-05-04 | 2017-03-15 | メルク パテント ゲゼルシャフト ミット ベシュレンクテル ハフツングＭｅｒｃｋ Ｐａｔｅｎｔ Ｇｅｓｅｌｌｓｃｈａｆｔ ｍｉｔ ｂｅｓｃｈｒａｅｎｋｔｅｒ Ｈａｆｔｕｎｇ | ピロロトリアジノン誘導体 |
| CN103450204B (zh) | 2012-05-31 | 2016-08-17 | 中国科学院上海药物研究所 | 吡咯[2，1-f][1，2，4]并三嗪类化合物，其制备方法及用途 |
| US9724352B2 (en) | 2012-05-31 | 2017-08-08 | Shanghai Institute Of Materia Medica, Chinese Academy Of Sciences | Pyrrolo[2,1-F[1,2,4]triazine compounds, preparation methods and applications thereof |
| WO2014143607A1 (en) * | 2013-03-11 | 2014-09-18 | Bristol-Myers Squibb Company | Pyrrolopyridazines as potassium ion channel inhibitors |
| US9050345B2 (en) | 2013-03-11 | 2015-06-09 | Bristol-Myers Squibb Company | Pyrrolotriazines as potassium ion channel inhibitors |
| EP2970294B1 (en) * | 2013-03-11 | 2016-12-28 | Bristol-Myers Squibb Company | Pyrrolotriazines as potassium ion channel inhibitors |
| ES2969565T3 (es) | 2015-09-30 | 2024-12-13 | Max Planck Ges Zur Foerderung Derwissenschaften E V | Derivados heteroarílicos como inhibidores de la sepiapterina reductasa |
| JP7114076B2 (ja) | 2015-12-22 | 2022-08-08 | シャイ・セラピューティクス・エルエルシー | がん及び炎症性疾患の処置のための化合物 |
| CN108341819B (zh) * | 2017-01-22 | 2021-06-15 | 南京药捷安康生物科技有限公司 | 磷酸二酯酶抑制剂及其用途 |
| CA3066939A1 (en) | 2017-06-21 | 2018-12-27 | SHY Therapeutics LLC | Compounds that interact with the ras superfamily for the treatment of cancers, inflammatory diseases, rasopathies, and fibrotic disease |
| EP3898609A1 (en) | 2018-12-19 | 2021-10-27 | Shy Therapeutics LLC | Compounds that interact with the ras superfamily for the treatment of cancers, inflammatory diseases, rasopathies, and fibrotic disease |
| EP4504341A1 (en) | 2022-04-08 | 2025-02-12 | Shy Therapeutics LLC | Compounds that interact with ras superfamily proteins for treatment of cancers, inflammatory diseases, rasopathies, and fibrotic disease |
Family Cites Families (10)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CZ303660B6 (cs) | 1999-05-21 | 2013-02-13 | Bristol-Myers Squibb Company | Pyrrolotriazin a farmaceutický prostredek s jeho obsahem |
| US6982265B1 (en) * | 1999-05-21 | 2006-01-03 | Bristol Myers Squibb Company | Pyrrolotriazine inhibitors of kinases |
| US6670357B2 (en) * | 2000-11-17 | 2003-12-30 | Bristol-Myers Squibb Company | Methods of treating p38 kinase-associated conditions and pyrrolotriazine compounds useful as kinase inhibitors |
| TWI329112B (en) * | 2002-07-19 | 2010-08-21 | Bristol Myers Squibb Co | Novel inhibitors of kinases |
| MXPA05008183A (es) * | 2003-02-05 | 2005-10-05 | Bristol Myers Squibb Co | Proceso para preparar pirrolotriazina como inhibidores de cinasa. |
| CA2520465A1 (en) * | 2003-03-28 | 2004-10-14 | Scios Inc. | Bi-cyclic pyrimidine inhibitors of tgf.beta. |
| AP2007003923A0 (en) | 2004-09-30 | 2007-02-28 | Tibotec Pharm Ltd | Hcv inhibiting bi-cyclic pyrimidines |
| DE602005023333D1 (de) | 2004-10-15 | 2010-10-14 | Takeda Pharmaceutical | Kinaseinhibitoren |
| CN101511835B (zh) * | 2006-07-07 | 2013-11-27 | 布里斯托尔-迈尔斯斯奎布公司 | 吡咯并三嗪激酶抑制剂 |
| US7531539B2 (en) * | 2006-08-09 | 2009-05-12 | Bristol-Myers Squibb Company | Pyrrolotriazine kinase inhibitors |
-
2008
- 2008-04-17 EP EP08780535A patent/EP2134716A1/en not_active Withdrawn
- 2008-04-17 JP JP2010504237A patent/JP5319659B2/ja not_active Expired - Fee Related
- 2008-04-17 US US12/596,058 patent/US8198438B2/en active Active
- 2008-04-17 CN CN2008800205589A patent/CN101687874B/zh not_active Expired - Fee Related
- 2008-04-17 WO PCT/US2008/060551 patent/WO2008131050A1/en not_active Ceased
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