JP2011507881A5 - - Google Patents
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- Publication number
- JP2011507881A5 JP2011507881A5 JP2010539781A JP2010539781A JP2011507881A5 JP 2011507881 A5 JP2011507881 A5 JP 2011507881A5 JP 2010539781 A JP2010539781 A JP 2010539781A JP 2010539781 A JP2010539781 A JP 2010539781A JP 2011507881 A5 JP2011507881 A5 JP 2011507881A5
- Authority
- JP
- Japan
- Prior art keywords
- aliphatic
- membered
- ring
- nhc
- compound according
- 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
- 125000001931 aliphatic group Chemical group 0.000 claims description 102
- 150000001875 compounds Chemical class 0.000 claims description 99
- 125000000623 heterocyclic group Chemical group 0.000 claims description 54
- 125000004429 atom Chemical group 0.000 claims description 52
- 229910052736 halogen Inorganic materials 0.000 claims description 40
- 150000002367 halogens Chemical class 0.000 claims description 40
- 125000002723 alicyclic group Chemical group 0.000 claims description 31
- 239000000203 mixture Substances 0.000 claims description 30
- 125000001424 substituent group Chemical group 0.000 claims description 28
- 125000003118 aryl group Chemical group 0.000 claims description 24
- 239000003814 drug Substances 0.000 claims description 24
- 229920006395 saturated elastomer Polymers 0.000 claims description 24
- 229910052739 hydrogen Inorganic materials 0.000 claims description 20
- 229940079593 drug Drugs 0.000 claims description 16
- 229910052799 carbon Inorganic materials 0.000 claims description 15
- 125000001313 C5-C10 heteroaryl group Chemical group 0.000 claims description 11
- 238000000034 method Methods 0.000 claims description 11
- 125000006570 (C5-C6) heteroaryl group Chemical group 0.000 claims description 10
- 125000001559 cyclopropyl group Chemical group [H]C1([H])C([H])([H])C1([H])* 0.000 claims description 10
- 229910052757 nitrogen Inorganic materials 0.000 claims description 10
- 125000006163 5-membered heteroaryl group Chemical group 0.000 claims description 8
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims description 8
- 125000001072 heteroaryl group Chemical group 0.000 claims description 8
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims description 8
- 229940124597 therapeutic agent Drugs 0.000 claims description 8
- 125000000325 methylidene group Chemical group [H]C([H])=* 0.000 claims description 7
- 125000006297 carbonyl amino group Chemical group [H]N([*:2])C([*:1])=O 0.000 claims description 6
- 125000002915 carbonyl group Chemical group [*:2]C([*:1])=O 0.000 claims description 6
- 150000003839 salts Chemical class 0.000 claims description 6
- 238000011282 treatment Methods 0.000 claims description 6
- OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical group [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 claims description 5
- 101000997832 Homo sapiens Tyrosine-protein kinase JAK2 Proteins 0.000 claims description 5
- 102100033444 Tyrosine-protein kinase JAK2 Human genes 0.000 claims description 5
- 125000001054 5 membered carbocyclic group Chemical group 0.000 claims description 4
- 125000003341 7 membered heterocyclic group Chemical group 0.000 claims description 4
- 208000024172 Cardiovascular disease Diseases 0.000 claims description 4
- 208000014767 Myeloproliferative disease Diseases 0.000 claims description 4
- 201000007224 Myeloproliferative neoplasm Diseases 0.000 claims description 4
- 230000000735 allogeneic effect Effects 0.000 claims description 4
- 239000012472 biological sample Substances 0.000 claims description 4
- 210000001772 blood platelet Anatomy 0.000 claims description 4
- 238000010322 bone marrow transplantation Methods 0.000 claims description 4
- 201000010099 disease Diseases 0.000 claims description 4
- 208000035475 disorder Diseases 0.000 claims description 4
- 239000002552 dosage form Substances 0.000 claims description 4
- 230000000694 effects Effects 0.000 claims description 4
- 229910052731 fluorine Inorganic materials 0.000 claims description 4
- 230000002401 inhibitory effect Effects 0.000 claims description 4
- 229910052760 oxygen Inorganic materials 0.000 claims description 4
- 238000011476 stem cell transplantation Methods 0.000 claims description 4
- 125000005330 8 membered heterocyclic group Chemical group 0.000 claims description 3
- 125000001153 fluoro group Chemical group F* 0.000 claims description 3
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 claims description 2
- 125000004008 6 membered carbocyclic group Chemical group 0.000 claims description 2
- 208000037398 BCR-ABL1 negative atypical chronic myeloid leukemia Diseases 0.000 claims description 2
- 208000032791 BCR-ABL1 positive chronic myelogenous leukemia Diseases 0.000 claims description 2
- 208000019838 Blood disease Diseases 0.000 claims description 2
- -1 CF 3 Inorganic materials 0.000 claims description 2
- 208000032027 Essential Thrombocythemia Diseases 0.000 claims description 2
- 208000000616 Hemoptysis Diseases 0.000 claims description 2
- 206010048643 Hypereosinophilic syndrome Diseases 0.000 claims description 2
- 206010028561 Myeloid metaplasia Diseases 0.000 claims description 2
- 208000033833 Myelomonocytic Chronic Leukemia Diseases 0.000 claims description 2
- 208000037538 Myelomonocytic Juvenile Leukemia Diseases 0.000 claims description 2
- 108010025020 Nerve Growth Factor Proteins 0.000 claims description 2
- 102000007072 Nerve Growth Factors Human genes 0.000 claims description 2
- NINIDFKCEFEMDL-UHFFFAOYSA-N Sulfur Chemical group [S] NINIDFKCEFEMDL-UHFFFAOYSA-N 0.000 claims description 2
- 201000008736 Systemic mastocytosis Diseases 0.000 claims description 2
- 208000017733 acquired polycythemia vera Diseases 0.000 claims description 2
- 239000002671 adjuvant Substances 0.000 claims description 2
- 125000000217 alkyl group Chemical group 0.000 claims description 2
- 208000007502 anemia Diseases 0.000 claims description 2
- 239000003242 anti bacterial agent Substances 0.000 claims description 2
- 229940124599 anti-inflammatory drug Drugs 0.000 claims description 2
- 229940088710 antibiotic agent Drugs 0.000 claims description 2
- 239000003443 antiviral agent Substances 0.000 claims description 2
- 238000002617 apheresis Methods 0.000 claims description 2
- QVGXLLKOCUKJST-UHFFFAOYSA-N atomic oxygen Chemical group [O] QVGXLLKOCUKJST-UHFFFAOYSA-N 0.000 claims description 2
- 201000004892 atypical chronic myeloid leukemia Diseases 0.000 claims description 2
- 210000000988 bone and bone Anatomy 0.000 claims description 2
- 239000003795 chemical substances by application Substances 0.000 claims description 2
- 229910052801 chlorine Inorganic materials 0.000 claims description 2
- 208000021668 chronic eosinophilic leukemia Diseases 0.000 claims description 2
- 201000010902 chronic myelomonocytic leukemia Diseases 0.000 claims description 2
- 230000006735 deficit Effects 0.000 claims description 2
- 230000001066 destructive effect Effects 0.000 claims description 2
- 206010012601 diabetes mellitus Diseases 0.000 claims description 2
- 238000000502 dialysis Methods 0.000 claims description 2
- 239000003937 drug carrier Substances 0.000 claims description 2
- 210000003743 erythrocyte Anatomy 0.000 claims description 2
- 125000001301 ethoxy group Chemical group [H]C([H])([H])C([H])([H])O* 0.000 claims description 2
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims description 2
- 208000014951 hematologic disease Diseases 0.000 claims description 2
- 208000018706 hematopoietic system disease Diseases 0.000 claims description 2
- 125000005842 heteroatom Chemical group 0.000 claims description 2
- 230000036039 immunity Effects 0.000 claims description 2
- 239000002955 immunomodulating agent Substances 0.000 claims description 2
- 229940121354 immunomodulator Drugs 0.000 claims description 2
- 229960003444 immunosuppressant agent Drugs 0.000 claims description 2
- 239000003018 immunosuppressive agent Substances 0.000 claims description 2
- 125000001449 isopropyl group Chemical group [H]C([H])([H])C([H])(*)C([H])([H])[H] 0.000 claims description 2
- 201000005992 juvenile myelomonocytic leukemia Diseases 0.000 claims description 2
- 208000017169 kidney disease Diseases 0.000 claims description 2
- 210000000265 leukocyte Anatomy 0.000 claims description 2
- 208000019423 liver disease Diseases 0.000 claims description 2
- 125000000956 methoxy group Chemical group [H]C([H])([H])O* 0.000 claims description 2
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims description 2
- 125000002950 monocyclic group Chemical group 0.000 claims description 2
- 206010028537 myelofibrosis Diseases 0.000 claims description 2
- 239000003900 neurotrophic factor Substances 0.000 claims description 2
- IJGRMHOSHXDMSA-UHFFFAOYSA-N nitrogen Substances N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims description 2
- QJGQUHMNIGDVPM-UHFFFAOYSA-N nitrogen group Chemical group [N] QJGQUHMNIGDVPM-UHFFFAOYSA-N 0.000 claims description 2
- 239000001301 oxygen Chemical group 0.000 claims description 2
- 235000016236 parenteral nutrition Nutrition 0.000 claims description 2
- 239000008194 pharmaceutical composition Substances 0.000 claims description 2
- 208000037244 polycythemia vera Diseases 0.000 claims description 2
- 208000003476 primary myelofibrosis Diseases 0.000 claims description 2
- 238000001959 radiotherapy Methods 0.000 claims description 2
- 210000000952 spleen Anatomy 0.000 claims description 2
- 229910052717 sulfur Chemical group 0.000 claims description 2
- 239000011593 sulfur Chemical group 0.000 claims description 2
- 239000003981 vehicle Substances 0.000 claims description 2
- 125000004438 haloalkoxy group Chemical group 0.000 claims 5
- 125000001188 haloalkyl group Chemical group 0.000 claims 5
- 125000004122 cyclic group Chemical group 0.000 claims 2
- 235000014113 dietary fatty acids Nutrition 0.000 claims 1
- 229930195729 fatty acid Natural products 0.000 claims 1
- 239000000194 fatty acid Substances 0.000 claims 1
- 150000004665 fatty acids Chemical class 0.000 claims 1
- 150000002222 fluorine compounds Chemical class 0.000 claims 1
- 125000004767 (C1-C4) haloalkoxy group Chemical group 0.000 description 5
- 125000004765 (C1-C4) haloalkyl group Chemical group 0.000 description 5
- 125000004043 oxo group Chemical group O=* 0.000 description 5
- 125000002373 5 membered heterocyclic group Chemical group 0.000 description 2
- 125000004070 6 membered heterocyclic group Chemical group 0.000 description 2
- 125000003627 8 membered carbocyclic group Chemical group 0.000 description 2
- 125000006714 (C3-C10) heterocyclyl group Chemical group 0.000 description 1
- 102000001253 Protein Kinase Human genes 0.000 description 1
- 229940124639 Selective inhibitor Drugs 0.000 description 1
- 235000019000 fluorine Nutrition 0.000 description 1
- 108060006633 protein kinase Proteins 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US1482407P | 2007-12-19 | 2007-12-19 | |
| US61/014,824 | 2007-12-19 | ||
| PCT/US2008/087362 WO2009085913A1 (en) | 2007-12-19 | 2008-12-18 | PYRAZOLO [1,5-a] PYRIMIDINES USEFUL AS JAK2 INHIBITORS |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2011507881A JP2011507881A (ja) | 2011-03-10 |
| JP2011507881A5 true JP2011507881A5 (https=) | 2013-01-31 |
| JP5587206B2 JP5587206B2 (ja) | 2014-09-10 |
Family
ID=40431839
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2010539781A Expired - Fee Related JP5587206B2 (ja) | 2007-12-19 | 2008-12-18 | ＪＡＫ２阻害剤として有用なピラゾロ［１，５−ａ］ピリミジン |
Country Status (13)
| Country | Link |
|---|---|
| US (1) | US8937064B2 (https=) |
| EP (1) | EP2252618A1 (https=) |
| JP (1) | JP5587206B2 (https=) |
| KR (1) | KR20100108390A (https=) |
| CN (1) | CN101932583A (https=) |
| AU (1) | AU2008343173A1 (https=) |
| CA (1) | CA2709710A1 (https=) |
| IL (1) | IL206466A0 (https=) |
| MX (1) | MX2010006748A (https=) |
| NZ (1) | NZ586662A (https=) |
| RU (1) | RU2010129928A (https=) |
| WO (1) | WO2009085913A1 (https=) |
| ZA (1) | ZA201004368B (https=) |
Families Citing this family (20)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| AR077999A1 (es) * | 2009-09-02 | 2011-10-05 | Vifor Int Ag | Antagonistas de pirimidin y triazin-hepcidina |
| EP2338888A1 (en) * | 2009-12-24 | 2011-06-29 | Almirall, S.A. | Imidazopyridine derivatives as JAK inhibitors |
| UY33213A (es) * | 2010-02-18 | 2011-09-30 | Almirall Sa | Derivados de pirazol como inhibidores de jak |
| WO2012044561A2 (en) * | 2010-09-30 | 2012-04-05 | Merck Sharp & Dohme Corp. | 2-alkoxy pyrimidine pde10 inhibitors |
| EP2463289A1 (en) | 2010-11-26 | 2012-06-13 | Almirall, S.A. | Imidazo[1,2-b]pyridazine derivatives as JAK inhibitors |
| EP2734205B1 (en) | 2011-07-21 | 2018-03-21 | Tolero Pharmaceuticals, Inc. | Heterocyclic protein kinase inhibitors |
| EP2554544A1 (en) | 2011-08-01 | 2013-02-06 | Almirall, S.A. | Pyridin-2(1h)-one derivatives as jak inhibitors |
| EP4556010A3 (en) | 2011-11-30 | 2025-07-23 | Emory University | Jak inhibitors for use in the prevention or treatment of a viral disease caused by a coronaviridae |
| CN102887858B (zh) * | 2012-09-07 | 2014-11-19 | 苏州康润医药有限公司 | 3-氯-5-氨基-1h-吡唑-4-甲酸乙酯的合成方法 |
| CN103073549A (zh) * | 2012-09-07 | 2013-05-01 | 苏州康润医药有限公司 | 3-溴吡唑啉[1,5-α]吡嘧啶-2-甲酸的合成工艺 |
| SI2941432T1 (en) * | 2012-12-07 | 2018-07-31 | Vertex Pharmaceuticals Incorporated | 2-AMINO-6-FLUORO-N- (5-FLUORO-4- (4- (4- (OXETHAN-3-YL) PIPERAZIN-1-CARBONYL) PIPERIDIN-1-YLIPRIDIN-3-YL) 1,5 ALFA) PYRIMIDINE-3-CARBOXAMIDE AS ATR KINAZE INHIBITOR |
| DK3077397T3 (da) | 2013-12-06 | 2019-12-16 | Vertex Pharma | 2-amino-6-fluor-n-[5-fluor-pyridin-3-yl]pyrazolo[1,5-a]pyrimidin-3-carboxamidforbindelse anvendelig som atr-kinase-inhibitor, dens fremstilling, forskellige faste former og radiomarkerede derivater deraf |
| WO2017013270A1 (en) | 2015-07-23 | 2017-01-26 | Universite De Strasbourg | Use of leptin signaling inhibitor for protecting kidneys from patients having ciliopathy |
| HK1258570A1 (zh) | 2015-09-30 | 2019-11-15 | Vertex Pharmaceuticals Inc. | 使用dna损伤剂及atr抑制剂的组合治疗癌症的方法 |
| CN117838695A (zh) | 2018-04-13 | 2024-04-09 | 住友制药肿瘤公司 | 用于治疗骨髓增殖性肿瘤和与癌症相关的纤维化的pim激酶抑制剂 |
| NZ778055A (en) | 2019-02-12 | 2025-11-28 | Sumitomo Pharma America Inc | Formulations comprising heterocyclic protein kinase inhibitors |
| CN114761013A (zh) | 2019-09-27 | 2022-07-15 | 迪斯克医药公司 | 治疗骨髓纤维化和相关病症的方法 |
| WO2021231798A1 (en) | 2020-05-13 | 2021-11-18 | Disc Medicine, Inc. | Anti-hemojuvelin (hjv) antibodies for treating myelofibrosis |
| EP4598539A2 (en) * | 2022-10-04 | 2025-08-13 | Children's Hospital Medical Center | Multi-cyclic irak and flt3 inhibiting compounds and uses thereof |
| EP4611753A1 (en) | 2022-10-31 | 2025-09-10 | Sumitomo Pharma America, Inc. | Pim1 inhibitor for treating myeloproliferative neoplasms |
Family Cites Families (20)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US5304121A (en) | 1990-12-28 | 1994-04-19 | Boston Scientific Corporation | Drug delivery system making use of a hydrogel polymer coating |
| US5886026A (en) | 1993-07-19 | 1999-03-23 | Angiotech Pharmaceuticals Inc. | Anti-angiogenic compositions and methods of use |
| US6099562A (en) | 1996-06-13 | 2000-08-08 | Schneider (Usa) Inc. | Drug coating with topcoat |
| IL127566A0 (en) | 1996-08-28 | 1999-10-28 | Pfizer | Substituted 6,5-hetero- bicyclic derivatives |
| CA2291709A1 (en) | 1997-05-30 | 1998-12-03 | Merck & Co., Inc. | Novel angiogenesis inhibitors |
| US6245759B1 (en) | 1999-03-11 | 2001-06-12 | Merck & Co., Inc. | Tyrosine kinase inhibitors |
| US7713989B2 (en) * | 2000-04-27 | 2010-05-11 | Dow Robert L | Glucocorticoid receptor modulators |
| GB0103926D0 (en) | 2001-02-17 | 2001-04-04 | Astrazeneca Ab | Chemical compounds |
| DK1532145T3 (da) | 2002-08-02 | 2007-01-15 | Vertex Pharma | Pyrazolpræparater der er anvendelige som inhibitorer af GSK-3 |
| US7550470B2 (en) | 2002-12-11 | 2009-06-23 | Merck & Co. Inc. | Substituted pyrazolo[1,5-A]pyrimidines as tyrosine kinase inhibitors |
| US7226919B2 (en) * | 2002-12-18 | 2007-06-05 | Vertex Pharmaceuticals Inc. | Compositions useful as inhibitors of protein kinases |
| NZ546058A (en) * | 2004-01-12 | 2010-09-30 | Ym Biosciences Australia Pty | Benzimidazole and other fused ring derivatives as selective janus kinase inhibitors |
| TWI372624B (en) * | 2004-03-30 | 2012-09-21 | Vertex Pharma | Azaindoles useful as inhibitors of jak and other protein kinases |
| GB0519957D0 (en) | 2005-09-30 | 2005-11-09 | Sb Pharmco Inc | Chemical compound |
| ATE482213T1 (de) * | 2004-11-04 | 2010-10-15 | Vertex Pharma | Als inhibitoren von proteinkinasen geeignete pyrazoloä1,5-aüpyrimidine |
| WO2007017678A1 (en) | 2005-08-09 | 2007-02-15 | Eirx Therapeutics Limited | Pyrazolo[1,5-a] pyrimidine compounds and pharmaceutical compositions containing them |
| ZA200802685B (en) * | 2005-09-30 | 2009-10-28 | Vertex Pharma | Deazapurines useful as inhibitors of janus kinases |
| CN101679409B (zh) * | 2006-12-22 | 2014-11-26 | Astex治疗学有限公司 | 双环杂环衍生化合物、其医药组合物和其用途 |
| ATE526328T1 (de) * | 2007-03-09 | 2011-10-15 | Vertex Pharma | Als inhibitoren von proteinkinasen geeignete aminopyrimidine |
| CN101790532B (zh) | 2007-07-31 | 2013-11-20 | 沃泰克斯药物股份有限公司 | 5-氟-1H-吡唑并[3，4-b]吡啶-3-胺及其衍生物的制备方法 |
-
2008
- 2008-12-18 NZ NZ586662A patent/NZ586662A/xx not_active IP Right Cessation
- 2008-12-18 JP JP2010539781A patent/JP5587206B2/ja not_active Expired - Fee Related
- 2008-12-18 RU RU2010129928/04A patent/RU2010129928A/ru not_active Application Discontinuation
- 2008-12-18 AU AU2008343173A patent/AU2008343173A1/en not_active Abandoned
- 2008-12-18 CA CA2709710A patent/CA2709710A1/en not_active Abandoned
- 2008-12-18 KR KR1020107015961A patent/KR20100108390A/ko not_active Withdrawn
- 2008-12-18 WO PCT/US2008/087362 patent/WO2009085913A1/en not_active Ceased
- 2008-12-18 EP EP08867722A patent/EP2252618A1/en not_active Withdrawn
- 2008-12-18 MX MX2010006748A patent/MX2010006748A/es unknown
- 2008-12-18 CN CN2008801260776A patent/CN101932583A/zh active Pending
-
2010
- 2010-06-17 US US12/817,785 patent/US8937064B2/en not_active Expired - Fee Related
- 2010-06-17 IL IL206466A patent/IL206466A0/en unknown
- 2010-06-21 ZA ZA2010/04368A patent/ZA201004368B/en unknown
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