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 (https=) | 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 (https=) |
| EP (1) | EP2061762B1 (https=) |
| JP (1) | JP5252404B2 (https=) |
| AT (1) | ATE517868T1 (https=) |
| CA (1) | CA2660560A1 (https=) |
| WO (1) | WO2008022164A2 (https=) |
Families Citing this family (43)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP2455382B1 (en) | 2005-12-13 | 2016-10-26 | Incyte Holdings Corporation | Heteroaryl substituted pyrrolo[2,3-b]pyridines and pyrrolo[2,3-b]pyrimidines as Janus kinase inhibitors |
| 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 |
| KR101599082B1 (ko) * | 2008-02-01 | 2016-03-02 | 어키니언 파마슈티칼스 아베 | 피라진 유도체 및 단백질 키나아제 억제제로서의 이의 용도 |
| JPWO2009153897A1 (ja) * | 2008-06-19 | 2011-11-24 | 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 |
| 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. |
| JP5775070B2 (ja) * | 2009-05-22 | 2015-09-09 | インサイト・コーポレイションＩｎｃｙｔｅ Ｃｏｒｐｏｒａｔｉｏｎ | ヤヌスキナーゼ阻害剤としてのピラゾール−４−イル−ピロロ［２，３−ｄ］ピリミジンおよびピロール−３−イル−ピロロ［２，３−ｄ］ピリミジンのＮ−（ヘテロ）アリール−ピロリジン誘導体 |
| SG176111A1 (en) * | 2009-05-22 | 2011-12-29 | Incyte Corp | 3-[4-(7h-pyrrolo[2,3-d]pyrimidin-4-yl)-1h-pyrazol-1-yl]octane- or heptane-nitrile as jak inhibitors |
| 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 |
| PT3354652T (pt) | 2010-03-10 | 2020-07-20 | Incyte Holdings Corp | Derivados de piperidin-4-ilazetidina como inibidores de jak1 |
| RS54824B1 (sr) | 2010-05-21 | 2016-10-31 | Incyte Holdings Corp | Topikalna formulacija za inhibiciju jak-a |
| CA2818542A1 (en) | 2010-11-19 | 2012-05-24 | Incyte Corporation | Cyclobutyl substituted pyrrolopyridine and pyrrolopyrimidine derivatives as jak inhibitors |
| WO2012068440A1 (en) | 2010-11-19 | 2012-05-24 | Incyte Corporation | Heterocyclic-substituted pyrrolopyridines and pyrrolopyrimidines as jak inhibitors |
| UY33930A (es) | 2011-03-04 | 2012-10-31 | Novartis Ag | Inhibidores novedosos de quinasas |
| WO2012120415A1 (en) | 2011-03-04 | 2012-09-13 | Novartis Ag | Tetrasubstituted cyclohexyl compounds as kinase inhibitors |
| MY165963A (en) | 2011-06-20 | 2018-05-18 | Incyte Holdings Corp | Azetidinyl phenyl, pyridyl or pyrazinyl carboxamide derivatives as jak inhibitors |
| 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 |
| US9173883B2 (en) | 2012-05-21 | 2015-11-03 | Novartis Ag | Ring-substituted N-pyridinyl amides as kinase inhibitors |
| 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 |
| CN113384546A (zh) | 2012-11-15 | 2021-09-14 | 因赛特公司 | 鲁索利替尼的缓释剂型 |
| 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 |
| RS60244B1 (sr) | 2013-01-15 | 2020-06-30 | Incyte Holdings Corp | Jedinjenja tiazolkarboksamida i piridinkarboksamida korisna kao inhibitori pim kinaze |
| WO2014138168A1 (en) | 2013-03-06 | 2014-09-12 | Incyte Corporation | Processes and intermediates for making a jak inhibitor |
| SG10201801069QA (en) | 2013-08-07 | 2018-03-28 | Incyte Corp | Sustained release dosage forms for a jak1 inhibitor |
| CN105658653A (zh) | 2013-08-23 | 2016-06-08 | 因赛特公司 | 可用作pim激酶抑制剂的呋喃并-和噻吩并-吡啶甲酰胺化合物 |
| 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 |
| US9580418B2 (en) | 2014-07-14 | 2017-02-28 | Incyte Corporation | Bicyclic aromatic carboxamide compounds useful as Pim kinase inhibitors |
| WO2016010897A1 (en) | 2014-07-14 | 2016-01-21 | Incyte Corporation | Bicyclic heteroaromatic carboxamide compounds useful as pim kinase inhibitors |
| WO2016196244A1 (en) | 2015-05-29 | 2016-12-08 | 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 |
| US11542256B2 (en) | 2017-09-03 | 2023-01-03 | Angion Biomedica Corp. | Vinylheterocycles as Rho-associated coiled-coil kinase (ROCK) inhibitors |
| AR113922A1 (es) | 2017-12-08 | 2020-07-01 | Incyte Corp | Terapia de combinación de dosis baja para el tratamiento de neoplasias mieloproliferativas |
| EA202091830A1 (ru) | 2018-01-30 | 2020-12-29 | Инсайт Корпорейшн | Способы и промежуточные соединения для получения ингибитора jak |
| MD3773593T2 (ro) | 2018-03-30 | 2024-10-31 | Incyte Corp | Tratament hidradenitei supurative utilizând inhibitori ai 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 |
|---|---|---|---|---|
| US20040102455A1 (en) * | 2001-01-30 | 2004-05-27 | Burns Christopher John | Method of inhibiting kinases |
| GB0119865D0 (en) * | 2001-08-14 | 2001-10-10 | Cancer Res Campaign Tech | DNA-PK inhibitors |
| US7015227B2 (en) * | 2002-06-21 | 2006-03-21 | Cgi Pharmaceuticals, Inc. | Certain amino-substituted monocycles as kinase modulators |
| WO2005026129A1 (en) * | 2003-09-15 | 2005-03-24 | Gpc Biotech Ag | Pharmaceutically active 4,6-disubstituted aminopyrimidine derivatives as modulators of protein kinases |
| CA2545422C (en) * | 2003-12-03 | 2015-06-02 | Cytopia Research Pty Ltd | Tubulin inhibitors |
| WO2005058876A1 (en) | 2003-12-16 | 2005-06-30 | Gpc Biotech Ag | Pyrazine derivatives as effective compounds against infectious diseases |
| EP1814856A1 (en) * | 2004-11-12 | 2007-08-08 | Galapagos N.V. | Nitrogen heteroaromatic compounds which bind to the active site of protein kinase enzymes |
| JP2009514876A (ja) * | 2005-11-03 | 2009-04-09 | アイアールエム・リミテッド・ライアビリティ・カンパニー | タンパク質キナーゼのための化合物および組成物 |
-
2007
- 2007-08-15 JP JP2009524774A patent/JP5252404B2/ja not_active Expired - Fee Related
- 2007-08-15 WO PCT/US2007/075946 patent/WO2008022164A2/en not_active Ceased
- 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 CA CA002660560A patent/CA2660560A1/en not_active Abandoned
- 2007-08-15 EP EP07800116A patent/EP2061762B1/en not_active Not-in-force