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
Links
- 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
- 125000006527 (C1-C5) alkyl group Chemical group 0.000 claims 12
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 11
- 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
- 125000003545 alkoxy 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
- 201000010099 disease Diseases 0.000 claims 7
- 125000000592 heterocycloalkyl group Chemical group 0.000 claims 7
- 150000003839 salts Chemical class 0.000 claims 7
- 239000011780 sodium chloride Substances 0.000 claims 7
- 230000001404 mediated 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 atoms Chemical group [H]* 0.000 claims 5
- 125000005842 heteroatoms Chemical group 0.000 claims 4
- 125000004433 nitrogen atoms Chemical group N* 0.000 claims 4
- 206010022114 Injury Diseases 0.000 claims 3
- 125000004183 alkoxy alkyl group Chemical group 0.000 claims 3
- 208000002193 Pain Diseases 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
- 125000005885 heterocycloalkylalkyl group Chemical group 0.000 claims 2
- 125000002768 hydroxyalkyl group Chemical group 0.000 claims 2
- 230000001575 pathological 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
- FILKGCRCWDMBKA-UHFFFAOYSA-N 2,6-dichloropyridine Chemical compound ClC1=CC=CC(Cl)=N1 FILKGCRCWDMBKA-UHFFFAOYSA-N 0.000 claims 1
- 208000005298 Acute Pain Diseases 0.000 claims 1
- 206010001897 Alzheimer's disease Diseases 0.000 claims 1
- 206010003210 Arteriosclerosis 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
- 206010008958 Chronic lymphocytic leukaemia Diseases 0.000 claims 1
- 210000003714 Granulocytes Anatomy 0.000 claims 1
- 208000002183 Guillain-Barre Syndrome Diseases 0.000 claims 1
- 206010061218 Inflammation Diseases 0.000 claims 1
- 208000000429 Leukemia, Lymphocytic, Chronic, B-Cell Diseases 0.000 claims 1
- 210000000265 Leukocytes Anatomy 0.000 claims 1
- 241000124008 Mammalia Species 0.000 claims 1
- 208000010125 Myocardial Infarction Diseases 0.000 claims 1
- 206010051606 Necrotising colitis Diseases 0.000 claims 1
- 208000004995 Necrotizing Enterocolitis Diseases 0.000 claims 1
- 206010029592 Non-Hodgkin's lymphomas Diseases 0.000 claims 1
- 206010035226 Plasma cell myeloma Diseases 0.000 claims 1
- 206010060862 Prostate cancer Diseases 0.000 claims 1
- 206010063837 Reperfusion injury Diseases 0.000 claims 1
- 238000006069 Suzuki reaction reaction Methods 0.000 claims 1
- 230000001154 acute Effects 0.000 claims 1
- 150000001412 amines Chemical class 0.000 claims 1
- 201000001320 atherosclerosis Diseases 0.000 claims 1
- 230000024279 bone resorption Effects 0.000 claims 1
- 201000006233 congestive heart failure Diseases 0.000 claims 1
- 238000007887 coronary angioplasty Methods 0.000 claims 1
- 238000010511 deprotection reaction Methods 0.000 claims 1
- 201000009910 diseases by infectious agent Diseases 0.000 claims 1
- 238000001631 haemodialysis Methods 0.000 claims 1
- 230000000322 hemodialysis Effects 0.000 claims 1
- 230000002757 inflammatory Effects 0.000 claims 1
- 230000004054 inflammatory process Effects 0.000 claims 1
- 201000009906 meningitis Diseases 0.000 claims 1
- 201000009251 multiple myeloma 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
- 200000000008 restenosis Diseases 0.000 claims 1
- 239000002904 solvent Substances 0.000 claims 1
- 201000010874 syndrome Diseases 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 (pt-PT) | 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 (pt-PT) |
| EP (1) | EP2061762B1 (pt-PT) |
| JP (1) | JP5252404B2 (pt-PT) |
| AT (1) | ATE517868T1 (pt-PT) |
| CA (1) | CA2660560A1 (pt-PT) |
| WO (1) | WO2008022164A2 (pt-PT) |
Families Citing this family (43)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN103214483B (zh) | 2005-12-13 | 2014-12-17 | 因塞特公司 | 作为两面神激酶抑制剂的杂芳基取代的吡咯并[2，3-b]吡啶和吡咯并[2，3-b]嘧啶 |
| EP2740731B1 (en) | 2007-06-13 | 2016-03-23 | Incyte Holdings Corporation | Crystalline salts of the janus kinase inhibitor (r)-3-(4-(7h-pyrrolo[2,3-d]pyrimidin-4-yl)-1h-pyrazol-1-yl)-3-cyclopentylpropanenitrile |
| US8436171B2 (en) * | 2008-02-01 | 2013-05-07 | Akinion Pharmaceuticals Ab | Amino substituted pyrazines as inhibitors or protein kinases |
| US20110124630A1 (en) * | 2008-06-19 | 2011-05-26 | Naofumi Mukaida | Stemonamide synthesis intermediate and pharmaceutical composition for prevention and/or treatment of cancer |
| 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 |
| US8987251B2 (en) | 2008-08-19 | 2015-03-24 | Array Biopharma Inc. | Triazolopyridine compounds as PIM kinase inhibitors |
| 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. |
| BRPI1012159B1 (pt) | 2009-05-22 | 2022-01-25 | Incyte Holdings Corporation | Compostos derivados de n-(hetero)aril-pirrolidina de pirazol-4-il-pirrolo[2,3-d] pirimidinas e pirrol-3-il-pirrolo[2,3-d] pirimidinas como inibidores de janus cinase, composições farmacêuticas compreendendo os referidos compostos e usos dos mesmos |
| DK2432472T3 (da) | 2009-05-22 | 2019-11-18 | Incyte Holdings Corp | 3-[4-(7h-pyrrolo[2,3-d]pyrimidin-4-yl)-1h-pyrazol-1-yl]octan- eller heptan-nitril som jak-inhibitorer |
| TW201113285A (en) | 2009-09-01 | 2011-04-16 | Incyte Corp | Heterocyclic derivatives of pyrazol-4-yl-pyrrolo[2,3-d]pyrimidines as janus kinase inhibitors |
| KR102283091B1 (ko) | 2010-03-10 | 2021-07-30 | 인사이트 홀딩스 코포레이션 | Ｊａｋ１ 저해제로서의 피페리딘４일 아제티딘 유도체 |
| EP2574168B9 (en) | 2010-05-21 | 2016-10-05 | Incyte Holdings Corporation | Topical formulation for a jak inhibitor |
| AR083933A1 (es) | 2010-11-19 | 2013-04-10 | Incyte Corp | Derivados de pirrolopiridina y pirrolopirimidina sustituidos con ciclobutilo como inhibidores de jak |
| 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 |
| US20120225061A1 (en) | 2011-03-04 | 2012-09-06 | Matthew Burger | Tetrasubstituted cyclohexyl compounds as kinase inhibitors |
| UY33930A (es) | 2011-03-04 | 2012-10-31 | Novartis Ag | Inhibidores novedosos de quinasas |
| CN103797010B (zh) | 2011-06-20 | 2016-02-24 | 因塞特控股公司 | 作为jak抑制剂的氮杂环丁烷基苯基、吡啶基或吡嗪基甲酰胺衍生物 |
| 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 |
| US9193733B2 (en) | 2012-05-18 | 2015-11-24 | Incyte Holdings Corporation | Piperidinylcyclobutyl substituted pyrrolopyridine and pyrrolopyrimidine derivatives as JAK inhibitors |
| KR20150013548A (ko) | 2012-05-21 | 2015-02-05 | 노파르티스 아게 | 키나제 억제제로서의 신규 고리-치환된 n-피리디닐 아미드 |
| WO2014033630A1 (en) | 2012-08-31 | 2014-03-06 | Novartis Ag | Novel aminothiazole carboxamides as kinase inhibitors |
| WO2014033631A1 (en) | 2012-08-31 | 2014-03-06 | Novartis Ag | N-(3-pyridyl) biarylamides as kinase inhibitors |
| CR20190073A (es) | 2012-11-15 | 2019-04-25 | Incyte Holdings Corp | FORMAS DE DOSIFICACIÓN DE RUXOLITINIB DE LIBERACIÓN SOTENIDA (Divisional 2015-265) |
| US20150336960A1 (en) | 2012-12-19 | 2015-11-26 | Novartis Ag | Aryl-substituted fused bicyclic pyridazine compounds |
| JP6437452B2 (ja) | 2013-01-14 | 2018-12-12 | 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二環式芳香族カルボキサミド化合物 |
| MX2015009057A (es) | 2013-01-15 | 2015-10-05 | Incyte Corp | Compuestos de tiazolcarboxamidas y piridinacarboxamida utiles como inhibidores de cinasa pim. |
| RS62867B1 (sr) | 2013-03-06 | 2022-02-28 | Incyte Holdings Corp | Postupci i intermedijeri za dobijanje inhibitora jak |
| EP3030227B1 (en) | 2013-08-07 | 2020-04-08 | Incyte Corporation | Sustained release dosage forms for a jak1 inhibitor |
| TW201605866A (zh) | 2013-08-23 | 2016-02-16 | 英塞特公司 | 可用作ｐｉｍ激酶抑制劑之呋喃并－及噻吩并－吡啶甲醯胺化合物 |
| JP6554480B2 (ja) * | 2014-03-18 | 2019-07-31 | エフ・ホフマン−ラ・ロシュ・アクチェンゲゼルシャフト | オキセパン−２−イル−ピラゾール−４−イル−ヘテロシクリル−カルボキサミド化合物と使用方法 |
| 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 |
| US9822124B2 (en) | 2014-07-14 | 2017-11-21 | Incyte Corporation | Bicyclic heteroaromatic carboxamide compounds useful as Pim kinase inhibitors |
| US9580418B2 (en) | 2014-07-14 | 2017-02-28 | Incyte Corporation | Bicyclic aromatic carboxamide compounds useful as Pim kinase inhibitors |
| US9540347B2 (en) | 2015-05-29 | 2017-01-10 | Incyte Corporation | Pyridineamine compounds useful as Pim kinase inhibitors |
| AR105967A1 (es) | 2015-09-09 | 2017-11-29 | Incyte Corp | Sales de un inhibidor de pim quinasa |
| WO2017059251A1 (en) | 2015-10-02 | 2017-04-06 | Incyte Corporation | Heterocyclic compounds useful as pim kinase inhibitors |
| WO2019046795A1 (en) * | 2017-09-03 | 2019-03-07 | Angion Biomedica Corp. | VINYL HETEROCYCLES AS INHIBITORS OF RHO (ROCK) ASSOCIATED BISPIRALIZED KINASE |
| AR113922A1 (es) | 2017-12-08 | 2020-07-01 | Incyte Corp | Terapia de combinación de dosis baja para el tratamiento de neoplasias mieloproliferativas |
| PE20211310A1 (es) | 2018-01-30 | 2021-07-22 | Incyte Corp | Procedimiento para la elaboracion de un recipiente de vidrio de sosa-cal a partir de materiales formadores de vidrio 100% reciclados y un recipiente de vidrio elaborado a partir de dicho procedimiento |
| JP2021519775A (ja) | 2018-03-30 | 2021-08-12 | インサイト・コーポレイションＩｎｃｙｔｅ Ｃｏｒｐｏｒａｔｉｏｎ | Ｊａｋ阻害剤を用いる化膿性汗腺炎の治療 |
| 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 |
|---|---|---|---|---|
| EP1363702A4 (en) | 2001-01-30 | 2007-08-22 | Cytopia Pty Ltd | PROCESS FOR INHIBITING KINASES |
| GB0119865D0 (en) * | 2001-08-14 | 2001-10-10 | Cancer Res Campaign Tech | DNA-PK inhibitors |
| AU2003249369A1 (en) * | 2002-06-21 | 2004-01-06 | 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 |
| ES2360703T3 (es) * | 2003-12-03 | 2011-06-08 | Ym Biosciences Australia Pty Ltd | Inhibidores de la tubulina. |
| EP1694670A1 (en) * | 2003-12-16 | 2006-08-30 | GPC Biotech AG | Pyrazine derivatives as effective compounds against infectious diseases |
| JP2008519814A (ja) * | 2004-11-12 | 2008-06-12 | ガラパゴス・ナムローゼ・フェンノートシャップ | プロテインキナーゼ酵素の活性部位と結合する窒素複素環式芳香族化合物 |
| KR20080053954A (ko) * | 2005-11-03 | 2008-06-16 | 아이알엠 엘엘씨 | 단백질 키나제 억제제 |
-
2007
- 2007-08-15 AT AT07800116T patent/ATE517868T1/de not_active IP Right Cessation
- 2007-08-15 CA CA002660560A patent/CA2660560A1/en not_active Abandoned
- 2007-08-15 EP EP07800116A patent/EP2061762B1/en not_active Not-in-force
- 2007-08-15 WO PCT/US2007/075946 patent/WO2008022164A2/en active Application Filing
- 2007-08-15 JP JP2009524774A patent/JP5252404B2/ja not_active Expired - Fee Related
- 2007-08-15 US US12/377,283 patent/US8318723B2/en active Active
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