JP2010501003A5 - - Google Patents
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- Publication number
- JP2010501003A5 JP2010501003A5 JP2009524774A JP2009524774A JP2010501003A5 JP 2010501003 A5 JP2010501003 A5 JP 2010501003A5 JP 2009524774 A JP2009524774 A JP 2009524774A JP 2009524774 A JP2009524774 A JP 2009524774A JP 2010501003 A5 JP2010501003 A5 JP 2010501003A5
- Authority
- JP
- Japan
- Prior art keywords
- alkyl
- hydroxyl
- alkoxy
- substituted
- optionally substituted
- 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
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- 125000004178 (C1-C4) alkyl group Chemical group 0.000 claims 14
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims 14
- 150000001875 compounds Chemical class 0.000 claims 13
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 13
- 125000006527 (C1-C5) alkyl group Chemical group 0.000 claims 12
- 125000003545 alkoxy group Chemical group 0.000 claims 12
- 229910052757 nitrogen Inorganic materials 0.000 claims 11
- 125000001797 benzyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])* 0.000 claims 10
- 125000006552 (C3-C8) cycloalkyl group Chemical group 0.000 claims 9
- 125000000592 heterocycloalkyl group Chemical group 0.000 claims 9
- 239000008194 pharmaceutical composition Substances 0.000 claims 9
- 125000003917 carbamoyl group Chemical class [H]N([H])C(*)=O 0.000 claims 7
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 7
- 150000003839 salts Chemical class 0.000 claims 7
- 201000010099 disease Diseases 0.000 claims 6
- 230000001404 mediated effect Effects 0.000 claims 6
- 125000001424 substituent group Chemical group 0.000 claims 6
- 125000006273 (C1-C3) alkyl group Chemical group 0.000 claims 5
- 125000002252 acyl group Chemical group 0.000 claims 5
- 229910052739 hydrogen Inorganic materials 0.000 claims 5
- 239000001257 hydrogen Substances 0.000 claims 5
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims 5
- 125000005842 heteroatom Chemical group 0.000 claims 4
- 125000004433 nitrogen atom Chemical group N* 0.000 claims 4
- 208000014674 injury Diseases 0.000 claims 3
- 238000000034 method Methods 0.000 claims 3
- FILKGCRCWDMBKA-UHFFFAOYSA-N 2,6-dichloropyridine Chemical compound ClC1=CC=CC(Cl)=N1 FILKGCRCWDMBKA-UHFFFAOYSA-N 0.000 claims 2
- 206010028980 Neoplasm Diseases 0.000 claims 2
- 208000002193 Pain Diseases 0.000 claims 2
- 208000027418 Wounds and injury Diseases 0.000 claims 2
- 230000001154 acute effect Effects 0.000 claims 2
- 125000000217 alkyl group Chemical group 0.000 claims 2
- 201000011510 cancer Diseases 0.000 claims 2
- 239000003153 chemical reaction reagent Substances 0.000 claims 2
- 230000006378 damage Effects 0.000 claims 2
- 230000001575 pathological effect Effects 0.000 claims 2
- LSEAAPGIZCDEEH-UHFFFAOYSA-N 2,6-dichloropyrazine Chemical compound ClC1=CN=CC(Cl)=N1 LSEAAPGIZCDEEH-UHFFFAOYSA-N 0.000 claims 1
- 208000024827 Alzheimer disease Diseases 0.000 claims 1
- 201000001320 Atherosclerosis Diseases 0.000 claims 1
- 208000010839 B-cell chronic lymphocytic leukemia Diseases 0.000 claims 1
- 208000006386 Bone Resorption Diseases 0.000 claims 1
- 206010007559 Cardiac failure congestive Diseases 0.000 claims 1
- 208000000094 Chronic Pain Diseases 0.000 claims 1
- 208000035895 Guillain-Barré syndrome Diseases 0.000 claims 1
- 206010019280 Heart failures Diseases 0.000 claims 1
- 206010061218 Inflammation Diseases 0.000 claims 1
- 208000031422 Lymphocytic Chronic B-Cell Leukemia Diseases 0.000 claims 1
- 241000124008 Mammalia Species 0.000 claims 1
- 201000009906 Meningitis Diseases 0.000 claims 1
- 206010049567 Miller Fisher syndrome Diseases 0.000 claims 1
- 208000034578 Multiple myelomas Diseases 0.000 claims 1
- 206010051606 Necrotising colitis Diseases 0.000 claims 1
- 208000015914 Non-Hodgkin lymphomas Diseases 0.000 claims 1
- 206010035226 Plasma cell myeloma Diseases 0.000 claims 1
- 206010060862 Prostate cancer Diseases 0.000 claims 1
- 208000000236 Prostatic Neoplasms Diseases 0.000 claims 1
- 206010063837 Reperfusion injury Diseases 0.000 claims 1
- 238000006069 Suzuki reaction reaction Methods 0.000 claims 1
- 208000005298 acute pain Diseases 0.000 claims 1
- 150000001412 amines Chemical class 0.000 claims 1
- 230000024279 bone resorption Effects 0.000 claims 1
- 208000032852 chronic lymphocytic leukemia Diseases 0.000 claims 1
- 238000007887 coronary angioplasty Methods 0.000 claims 1
- 238000010511 deprotection reaction Methods 0.000 claims 1
- 208000035475 disorder Diseases 0.000 claims 1
- 210000003714 granulocyte Anatomy 0.000 claims 1
- 238000001631 haemodialysis Methods 0.000 claims 1
- 230000000322 hemodialysis Effects 0.000 claims 1
- 208000015181 infectious disease Diseases 0.000 claims 1
- 230000002757 inflammatory effect Effects 0.000 claims 1
- 230000004054 inflammatory process Effects 0.000 claims 1
- 210000000265 leukocyte Anatomy 0.000 claims 1
- 208000010125 myocardial infarction Diseases 0.000 claims 1
- 208000004995 necrotizing enterocolitis Diseases 0.000 claims 1
- 201000008482 osteoarthritis Diseases 0.000 claims 1
- 201000006195 perinatal necrotizing enterocolitis Diseases 0.000 claims 1
- 238000009256 replacement therapy Methods 0.000 claims 1
- 208000037803 restenosis Diseases 0.000 claims 1
- 239000002904 solvent Substances 0.000 claims 1
- 208000011580 syndromic disease Diseases 0.000 claims 1
- 230000008733 trauma Effects 0.000 claims 1
- 238000011282 treatment Methods 0.000 claims 1
- URUQZMBSURPJJV-NSCUHMNNSA-N C/C=C/C(NCCO)=O Chemical compound C/C=C/C(NCCO)=O URUQZMBSURPJJV-NSCUHMNNSA-N 0.000 description 1
- CUPVPXAUGMDDMU-ONEGZZNKSA-N C/C=C/C(NS(C)(=O)=O)=O Chemical compound C/C=C/C(NS(C)(=O)=O)=O CUPVPXAUGMDDMU-ONEGZZNKSA-N 0.000 description 1
- LIXGZTCKAZKTPB-NSCUHMNNSA-N C/C=C/c1nnn[nH]1 Chemical compound C/C=C/c1nnn[nH]1 LIXGZTCKAZKTPB-NSCUHMNNSA-N 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US82254606P | 2006-08-16 | 2006-08-16 | |
| US60/822,546 | 2006-08-16 | ||
| PCT/US2007/075946 WO2008022164A2 (en) | 2006-08-16 | 2007-08-15 | Pyrazine compounds, their use and methods of preparation |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2010501003A JP2010501003A (ja) | 2010-01-14 |
| JP2010501003A5 true JP2010501003A5 (show.php) | 2010-09-30 |
| JP5252404B2 JP5252404B2 (ja) | 2013-07-31 |
Family
ID=38988263
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2009524774A Expired - Fee Related JP5252404B2 (ja) | 2006-08-16 | 2007-08-15 | ピラジン化合物、その使用及び調製方法 |
Country Status (6)
| Country | Link |
|---|---|
| US (1) | US8318723B2 (show.php) |
| EP (1) | EP2061762B1 (show.php) |
| JP (1) | JP5252404B2 (show.php) |
| AT (1) | ATE517868T1 (show.php) |
| CA (1) | CA2660560A1 (show.php) |
| WO (1) | WO2008022164A2 (show.php) |
Families Citing this family (43)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| HUE025173T2 (hu) | 2005-12-13 | 2016-01-28 | Incyte Corp | Heteroaril-szubsztituált pirrollo[2,3-b]piridinek és pirrolo[2,3-b]pirimidinek mint Janus-kináz inhibitorok |
| EP3070090B1 (en) | 2007-06-13 | 2018-12-12 | Incyte Holdings Corporation | Use of salts of the janus kinase inhibitor (r)-3-(4-(7h-pyrrolo[2,3-d]pyrimidin-4-yl)-1h- pyrazol-1-yl)-3- cyclopentylpropanenitrile |
| BRPI0907453A2 (pt) * | 2008-02-01 | 2015-07-14 | Akinion Pharmaceuticals Ab | Compostos, uso e preparação dos mesmos |
| WO2009153897A1 (ja) * | 2008-06-19 | 2009-12-23 | 国立大学法人金沢大学 | ステモナミド合成中間体ならびにがんを予防および／または治療するための医薬組成物 |
| US8987251B2 (en) | 2008-08-19 | 2015-03-24 | Array Biopharma Inc. | Triazolopyridine compounds as PIM kinase inhibitors |
| TWI496779B (zh) * | 2008-08-19 | 2015-08-21 | Array Biopharma Inc | 作為ｐｉｍ激酶抑制劑之三唑吡啶化合物 |
| CL2009001884A1 (es) * | 2008-10-02 | 2010-05-14 | Incyte Holdings Corp | Uso de 3-ciclopentil-3-[4-(7h-pirrolo[2,3-d]pirimidin-4-il)-1h-pirazol-1-il)propanonitrilo, inhibidor de janus quinasa, y uso de una composición que lo comprende para el tratamiento del ojo seco. |
| TW201100429A (en) | 2009-05-22 | 2011-01-01 | Incyte Corp | N-(hetero)aryl-pyrrolidine derivatives of pyrazol-4-yl-pyrrolo[2,3-d]pyrimidines and pyrrol-3-yl-pyrrolo[2,3-d]pyrimidines as janus kinase inhibitors |
| LT2432472T (lt) | 2009-05-22 | 2020-02-10 | Incyte Holdings Corporation | 3-[4-(7h-pirolo[2,3-d]pirimidin-4-il)-1h-pirazol-1-il]oktan- arba heptan-nitrilas, kaip jak inhibitoriai |
| AR078012A1 (es) | 2009-09-01 | 2011-10-05 | Incyte Corp | Derivados heterociclicos de las pirazol-4-il- pirrolo (2,3-d) pirimidinas como inhibidores de la quinasa janus |
| CA2792508C (en) | 2010-03-10 | 2018-01-16 | Incyte Corporation | Piperidin-4-yl azetidine derivatives as jak1 inhibitors |
| TWI499421B (zh) | 2010-05-21 | 2015-09-11 | Incyte Corp | Ｊａｋ抑制劑的局部製劑 |
| JP5917544B2 (ja) | 2010-11-19 | 2016-05-18 | インサイト・ホールディングス・コーポレイションＩｎｃｙｔｅ Ｈｏｌｄｉｎｇｓ Ｃｏｒｐｏｒａｔｉｏｎ | Ｊａｋ阻害剤としての複素環置換ピロロピリジンおよびピロロピリミジン |
| AU2011329734B2 (en) | 2010-11-19 | 2015-05-28 | Incyte Holdings Corporation | Cyclobutyl substituted pyrrolopyridine and pyrrolopyrimidine derivatives as JAK inhibitors |
| UY33930A (es) | 2011-03-04 | 2012-10-31 | Novartis Ag | Inhibidores novedosos de quinasas |
| CN103429572A (zh) | 2011-03-04 | 2013-12-04 | 诺瓦提斯公司 | 作为激酶抑制剂的四取代的环己基化合物 |
| ES2560611T3 (es) | 2011-06-20 | 2016-02-22 | Incyte Holdings Corporation | Derivados de fenil de azetidinilo, carboxamida de piridilo o pirazinilo como inhibidores de JAK |
| TW201313721A (zh) | 2011-08-18 | 2013-04-01 | Incyte Corp | 作為ｊａｋ抑制劑之環己基氮雜環丁烷衍生物 |
| UA111854C2 (uk) | 2011-09-07 | 2016-06-24 | Інсайт Холдінгс Корпорейшн | Способи і проміжні сполуки для отримання інгібіторів jak |
| TW201406761A (zh) | 2012-05-18 | 2014-02-16 | Incyte Corp | 做爲ｊａｋ抑制劑之哌啶基環丁基取代之吡咯并吡啶及吡咯并嘧啶衍生物 |
| TW201408641A (zh) | 2012-05-21 | 2014-03-01 | Novartis Ag | 可作爲激酶抑制劑之新穎環取代ｎ－吡啶基醯胺 |
| WO2014033631A1 (en) | 2012-08-31 | 2014-03-06 | Novartis Ag | N-(3-pyridyl) biarylamides as kinase inhibitors |
| WO2014033630A1 (en) | 2012-08-31 | 2014-03-06 | Novartis Ag | Novel aminothiazole carboxamides as kinase inhibitors |
| SG10202111768XA (en) | 2012-11-15 | 2021-11-29 | Incyte Holdings Corp | Sustained-release dosage forms of ruxolitinib |
| US20150336960A1 (en) | 2012-12-19 | 2015-11-26 | Novartis Ag | Aryl-substituted fused bicyclic pyridazine compounds |
| ES2649156T3 (es) | 2013-01-14 | 2018-01-10 | Incyte Holdings Corporation | Compuestos bicíclicos de carboxamida aromática útiles como inhibidores de quinasas Pim |
| JP6554037B2 (ja) | 2013-01-15 | 2019-07-31 | インサイト・ホールディングス・コーポレイションＩｎｃｙｔｅ Ｈｏｌｄｉｎｇｓ Ｃｏｒｐｏｒａｔｉｏｎ | Ｐｉｍキナーゼ阻害剤として有用なチアゾールカルボキサミドおよびピリジンカルボキサミド化合物 |
| PE20200298A1 (es) | 2013-03-06 | 2020-02-06 | Incyte Holdings Corp | Procesos e intermedios para hacer un inhibidor de jak |
| CN114010611B (zh) | 2013-08-07 | 2023-11-28 | 因赛特控股公司 | Jak1抑制剂的持续释放剂型 |
| AR097431A1 (es) | 2013-08-23 | 2016-03-16 | Incyte Corp | Compuestos de carboxamida de furo y tienopiridina útiles como inhibidores de quinasas pim |
| WO2015140189A1 (en) * | 2014-03-18 | 2015-09-24 | F. Hoffmann-La Roche Ag | Oxepan-2-yl-pyrazol-4-yl-heterocyclyl-carboxamide compounds and methods of use |
| US9498467B2 (en) | 2014-05-30 | 2016-11-22 | Incyte Corporation | Treatment of chronic neutrophilic leukemia (CNL) and atypical chronic myeloid leukemia (aCML) by inhibitors of JAK1 |
| US9580418B2 (en) | 2014-07-14 | 2017-02-28 | Incyte Corporation | Bicyclic aromatic carboxamide compounds useful as Pim kinase inhibitors |
| US9822124B2 (en) | 2014-07-14 | 2017-11-21 | Incyte Corporation | Bicyclic heteroaromatic carboxamide compounds useful as Pim kinase inhibitors |
| US9540347B2 (en) | 2015-05-29 | 2017-01-10 | Incyte Corporation | Pyridineamine compounds useful as Pim kinase inhibitors |
| TWI734699B (zh) | 2015-09-09 | 2021-08-01 | 美商英塞特公司 | Ｐｉｍ激酶抑制劑之鹽 |
| US9920032B2 (en) | 2015-10-02 | 2018-03-20 | Incyte Corporation | Heterocyclic compounds useful as pim kinase inhibitors |
| EP3676262A4 (en) | 2017-09-03 | 2021-03-31 | Angion Biomedica Corp. | VINYLHETEROCYCLENE AS RHO-ASSOCIATED COILED COIL KINASE (ROCK) INHIBITORS |
| TW201924683A (zh) | 2017-12-08 | 2019-07-01 | 美商英塞特公司 | 用於治療骨髓增生性贅瘤的低劑量組合療法 |
| RS63312B1 (sr) | 2018-01-30 | 2022-07-29 | Incyte Corp | Procesi za pripremu (1-(3-fluoro-2-(trifluorometil)izonikotinil)piperidin-4-on) |
| MX2020010322A (es) | 2018-03-30 | 2022-11-30 | Incyte Corp | Tratamiento de la hidradenitis supurativa mediante el uso de inhibidores de actividad de la cinasa janus (jak). |
| WO2020210428A1 (en) * | 2019-04-09 | 2020-10-15 | Baylor College Of Medicine | Novel inhibitors of flavivirus protease for prevention and treatment of zika, dengue and other flavivirus infections |
| US11833155B2 (en) | 2020-06-03 | 2023-12-05 | Incyte Corporation | Combination therapy for treatment of myeloproliferative neoplasms |
Family Cites Families (8)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2002060492A1 (en) * | 2001-01-30 | 2002-08-08 | Cytopia Pty Ltd | Methods of inhibiting kinases |
| GB0119865D0 (en) * | 2001-08-14 | 2001-10-10 | Cancer Res Campaign Tech | DNA-PK inhibitors |
| WO2004000318A2 (en) * | 2002-06-21 | 2003-12-31 | Cellular Genomics, Inc. | Certain amino-substituted monocycles as kinase modulators |
| EP1678147B1 (en) * | 2003-09-15 | 2012-08-08 | Lead Discovery Center GmbH | Pharmaceutically active 4,6-disubstituted aminopyrimidine derivatives as modulators of protein kinases |
| PT2277865E (pt) * | 2003-12-03 | 2015-02-05 | Ym Biosciences Australia Pty | Heterociclos de azoto de anel de 6 membros fenil substituídos como inibidores de polimerização de microtúbulos |
| WO2005058876A1 (en) * | 2003-12-16 | 2005-06-30 | Gpc Biotech Ag | Pyrazine derivatives as effective compounds against infectious diseases |
| WO2006051311A1 (en) * | 2004-11-12 | 2006-05-18 | Galapagos Nv | Nitrogen heteroaromatic compounds which bind to the active site of protein kinase enzymes |
| KR20080053954A (ko) * | 2005-11-03 | 2008-06-16 | 아이알엠 엘엘씨 | 단백질 키나제 억제제 |
-
2007
- 2007-08-15 WO PCT/US2007/075946 patent/WO2008022164A2/en not_active Ceased
- 2007-08-15 CA CA002660560A patent/CA2660560A1/en not_active Abandoned
- 2007-08-15 US US12/377,283 patent/US8318723B2/en active Active
- 2007-08-15 AT AT07800116T patent/ATE517868T1/de not_active IP Right Cessation
- 2007-08-15 JP JP2009524774A patent/JP5252404B2/ja not_active Expired - Fee Related
- 2007-08-15 EP EP07800116A patent/EP2061762B1/en not_active Not-in-force