JP2013010793A5 - - Google Patents
Download PDFInfo
- Publication number
- JP2013010793A5 JP2013010793A5 JP2012226368A JP2012226368A JP2013010793A5 JP 2013010793 A5 JP2013010793 A5 JP 2013010793A5 JP 2012226368 A JP2012226368 A JP 2012226368A JP 2012226368 A JP2012226368 A JP 2012226368A JP 2013010793 A5 JP2013010793 A5 JP 2013010793A5
- Authority
- JP
- Japan
- Prior art keywords
- pharmaceutically acceptable
- acceptable salt
- aliphatic
- unsubstituted
- compound
- 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.)
- Ceased
Links
- 150000001875 compounds Chemical class 0.000 claims description 51
- 125000001931 aliphatic group Chemical group 0.000 claims description 38
- 229910052739 hydrogen Inorganic materials 0.000 claims description 20
- 239000001257 hydrogen Substances 0.000 claims description 17
- 229910052736 halogen Inorganic materials 0.000 claims description 7
- 150000002367 halogens Chemical class 0.000 claims description 7
- 125000000623 heterocyclic group Chemical group 0.000 claims description 7
- 125000003118 aryl group Chemical group 0.000 claims description 6
- 125000001072 heteroaryl group Chemical group 0.000 claims description 6
- 125000001424 substituent group Chemical group 0.000 claims description 6
- -1 COOR ′ Chemical group 0.000 claims description 4
- 125000004429 atom Chemical group 0.000 claims description 2
- 125000004432 carbon atom Chemical group C* 0.000 claims description 2
- 239000000203 mixture Substances 0.000 claims description 2
- 229910052757 nitrogen Inorganic materials 0.000 claims description 2
- 150000003839 salts Chemical class 0.000 claims 48
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 9
- 229910052799 carbon Inorganic materials 0.000 claims 9
- 229910052731 fluorine Inorganic materials 0.000 claims 9
- 125000000325 methylidene group Chemical group [H]C([H])=* 0.000 claims 9
- 150000001721 carbon Chemical group 0.000 claims 7
- 150000002431 hydrogen Chemical class 0.000 claims 7
- 238000006467 substitution reaction Methods 0.000 claims 7
- PXGOKWXKJXAPGV-UHFFFAOYSA-N Fluorine Chemical compound FF PXGOKWXKJXAPGV-UHFFFAOYSA-N 0.000 claims 6
- 239000011737 fluorine Substances 0.000 claims 6
- 125000000217 alkyl group Chemical group 0.000 claims 5
- 239000003795 chemical substances by application Substances 0.000 claims 5
- 125000002837 carbocyclic group Chemical group 0.000 claims 4
- 229920006395 saturated elastomer Polymers 0.000 claims 4
- 229910052801 chlorine Inorganic materials 0.000 claims 3
- 239000000460 chlorine Substances 0.000 claims 3
- 125000001559 cyclopropyl group Chemical group [H]C1([H])C([H])([H])C1([H])* 0.000 claims 3
- 239000003814 drug Substances 0.000 claims 3
- 125000000896 monocarboxylic acid group Chemical group 0.000 claims 3
- OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical group [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 claims 2
- ZAMOUSCENKQFHK-UHFFFAOYSA-N Chlorine atom Chemical compound [Cl] ZAMOUSCENKQFHK-UHFFFAOYSA-N 0.000 claims 2
- 239000012472 biological sample Substances 0.000 claims 2
- 125000006297 carbonyl amino group Chemical group [H]N([*:2])C([*:1])=O 0.000 claims 2
- 229940079593 drug Drugs 0.000 claims 2
- 230000000694 effects Effects 0.000 claims 2
- 230000002401 inhibitory effect Effects 0.000 claims 2
- 125000006592 (C2-C3) alkenyl group Chemical group 0.000 claims 1
- 208000019838 Blood disease Diseases 0.000 claims 1
- 208000020084 Bone disease Diseases 0.000 claims 1
- 208000024172 Cardiovascular disease Diseases 0.000 claims 1
- JNCMHMUGTWEVOZ-UHFFFAOYSA-N F[CH]F Chemical compound F[CH]F JNCMHMUGTWEVOZ-UHFFFAOYSA-N 0.000 claims 1
- 108010081348 HRT1 protein Hairy Proteins 0.000 claims 1
- 102100021881 Hairy/enhancer-of-split related with YRPW motif protein 1 Human genes 0.000 claims 1
- 208000029462 Immunodeficiency disease Diseases 0.000 claims 1
- 108010025020 Nerve Growth Factor Proteins 0.000 claims 1
- 102000007072 Nerve Growth Factors Human genes 0.000 claims 1
- 239000002671 adjuvant Substances 0.000 claims 1
- 125000002723 alicyclic group Chemical group 0.000 claims 1
- 125000003342 alkenyl group Chemical group 0.000 claims 1
- 125000000304 alkynyl group Chemical group 0.000 claims 1
- 239000002260 anti-inflammatory agent Substances 0.000 claims 1
- 229940121363 anti-inflammatory agent Drugs 0.000 claims 1
- 230000001028 anti-proliverative effect Effects 0.000 claims 1
- 239000002246 antineoplastic agent Substances 0.000 claims 1
- 239000003443 antiviral agent Substances 0.000 claims 1
- 229940121357 antivirals Drugs 0.000 claims 1
- 238000006243 chemical reaction Methods 0.000 claims 1
- 229940044683 chemotherapy drug Drugs 0.000 claims 1
- 230000001066 destructive effect Effects 0.000 claims 1
- 206010012601 diabetes mellitus Diseases 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 210000002816 gill Anatomy 0.000 claims 1
- 208000014951 hematologic disease Diseases 0.000 claims 1
- 208000018706 hematopoietic system disease Diseases 0.000 claims 1
- 239000002955 immunomodulating agent Substances 0.000 claims 1
- 229940121354 immunomodulator Drugs 0.000 claims 1
- 229960003444 immunosuppressant agent Drugs 0.000 claims 1
- 239000003018 immunosuppressive agent Substances 0.000 claims 1
- 238000000338 in vitro Methods 0.000 claims 1
- 208000019423 liver disease Diseases 0.000 claims 1
- 238000000034 method Methods 0.000 claims 1
- 239000003900 neurotrophic factor Substances 0.000 claims 1
- 239000008194 pharmaceutical composition Substances 0.000 claims 1
- 239000000546 pharmaceutical excipient Substances 0.000 claims 1
- 150000003254 radicals Chemical class 0.000 claims 1
- 229940124597 therapeutic agent Drugs 0.000 claims 1
- 229910052760 oxygen Inorganic materials 0.000 description 3
- 125000005843 halogen group Chemical group 0.000 description 2
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 description 2
- 125000006570 (C5-C6) heteroaryl group Chemical group 0.000 description 1
- HBAQYPYDRFILMT-UHFFFAOYSA-N 8-[3-(1-cyclopropylpyrazol-4-yl)-1H-pyrazolo[4,3-d]pyrimidin-5-yl]-3-methyl-3,8-diazabicyclo[3.2.1]octan-2-one Chemical class C1(CC1)N1N=CC(=C1)C1=NNC2=C1N=C(N=C2)N1C2C(N(CC1CC2)C)=O HBAQYPYDRFILMT-UHFFFAOYSA-N 0.000 description 1
- NINIDFKCEFEMDL-UHFFFAOYSA-N Sulfur Chemical group [S] NINIDFKCEFEMDL-UHFFFAOYSA-N 0.000 description 1
- QVGXLLKOCUKJST-UHFFFAOYSA-N atomic oxygen Chemical group [O] QVGXLLKOCUKJST-UHFFFAOYSA-N 0.000 description 1
- 125000000753 cycloalkyl group Chemical group 0.000 description 1
- 125000005842 heteroatom Chemical group 0.000 description 1
- 125000004435 hydrogen atom Chemical class [H]* 0.000 description 1
- IJGRMHOSHXDMSA-UHFFFAOYSA-N nitrogen Substances N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 description 1
- QJGQUHMNIGDVPM-UHFFFAOYSA-N nitrogen group Chemical group [N] QJGQUHMNIGDVPM-UHFFFAOYSA-N 0.000 description 1
- 239000001301 oxygen Chemical group 0.000 description 1
- 229910052717 sulfur Chemical group 0.000 description 1
- 239000011593 sulfur Chemical group 0.000 description 1
Applications Claiming Priority (4)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US75936706P | 2006-01-17 | 2006-01-17 | |
| US60/759,367 | 2006-01-17 | ||
| US84247106P | 2006-09-06 | 2006-09-06 | |
| US60/842,471 | 2006-09-06 |
Related Parent Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2008551353A Division JP5591471B2 (ja) | 2006-01-17 | 2007-01-17 | ヤヌスキナーゼ阻害剤として有用なアザインドール |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2013010793A JP2013010793A (ja) | 2013-01-17 |
| JP2013010793A5 true JP2013010793A5 (enExample) | 2014-07-10 |
Family
ID=38197739
Family Applications (4)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2008551353A Expired - Fee Related JP5591471B2 (ja) | 2006-01-17 | 2007-01-17 | ヤヌスキナーゼ阻害剤として有用なアザインドール |
| JP2012226368A Ceased JP2013010793A (ja) | 2006-01-17 | 2012-10-11 | ヤヌスキナーゼ阻害剤として有用なアザインドール |
| JP2012226367A Expired - Fee Related JP5728454B2 (ja) | 2006-01-17 | 2012-10-11 | ヤヌスキナーゼ阻害剤として有用なアザインドール |
| JP2014167160A Pending JP2014210823A (ja) | 2006-01-17 | 2014-08-20 | ヤヌスキナーゼ阻害剤として有用なアザインドール |
Family Applications Before (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2008551353A Expired - Fee Related JP5591471B2 (ja) | 2006-01-17 | 2007-01-17 | ヤヌスキナーゼ阻害剤として有用なアザインドール |
Family Applications After (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2012226367A Expired - Fee Related JP5728454B2 (ja) | 2006-01-17 | 2012-10-11 | ヤヌスキナーゼ阻害剤として有用なアザインドール |
| JP2014167160A Pending JP2014210823A (ja) | 2006-01-17 | 2014-08-20 | ヤヌスキナーゼ阻害剤として有用なアザインドール |
Country Status (19)
| Country | Link |
|---|---|
| US (6) | US7767816B2 (enExample) |
| EP (3) | EP2537849A3 (enExample) |
| JP (4) | JP5591471B2 (enExample) |
| KR (3) | KR20130041313A (enExample) |
| CN (3) | CN102532134A (enExample) |
| AR (1) | AR060316A1 (enExample) |
| AU (1) | AU2007207533B8 (enExample) |
| BR (2) | BRPI0722364A2 (enExample) |
| CA (1) | CA2636189A1 (enExample) |
| CL (1) | CL2008002140A1 (enExample) |
| HK (1) | HK1210780A1 (enExample) |
| IL (1) | IL191902A0 (enExample) |
| NO (1) | NO20083501L (enExample) |
| NZ (3) | NZ592968A (enExample) |
| RU (2) | RU2453548C2 (enExample) |
| TW (4) | TWI423976B (enExample) |
| UA (1) | UA95940C2 (enExample) |
| WO (1) | WO2007084557A2 (enExample) |
| ZA (2) | ZA200805053B (enExample) |
Families Citing this family (105)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| ES2364340T3 (es) | 2004-03-30 | 2011-08-31 | Vertex Pharmaceuticals Incorporated | Azaindoles útiles como inhibidores de jak y otras proteína quinasas. |
| JP2008545660A (ja) * | 2005-05-20 | 2008-12-18 | バーテックス ファーマシューティカルズ インコーポレイテッド | プロテインキナーゼ阻害剤として有用なピロロピリジン化合物 |
| WO2007038215A1 (en) | 2005-09-22 | 2007-04-05 | Incyte Corporation | Tetracyclic inhibitors of janus kinases |
| HUE028588T2 (hu) | 2005-12-13 | 2016-12-28 | Incyte Holdings Corp | Heteroaril-szubsztituált pirrolo[2,3-b]piridinek és pirrolo[2,3-b]pirimidinek mint Janus-kináz inhibitorok |
| NZ592968A (en) | 2006-01-17 | 2012-08-31 | Vertex Pharma | Azaindoles substituted with either triazine or pyrimidine useful as inhibitors of janus kinases consisting of JAK1, JAK2, JAK3, and TYK2 |
| JP2009532475A (ja) * | 2006-04-05 | 2009-09-10 | バーテックス ファーマシューティカルズ インコーポレイテッド | ヤヌスキナーゼの阻害剤として有用なデアザプリン |
| US7754838B2 (en) * | 2006-08-08 | 2010-07-13 | E.I. Du Pont De Nemours And Company | Poly(meth)acrylamides and poly(meth)acrylates containing fluorinated amide |
| WO2008079346A1 (en) | 2006-12-21 | 2008-07-03 | Vertex Pharmaceuticals Incorporated | 5-cyan0-4- (pyrrolo [2, 3b] pyridine-3-yl) -pyrimidine derivatives useful as protein kinase inhibitors |
| ES2415863T3 (es) | 2006-12-22 | 2013-07-29 | Incyte Corporation | Heterociclos sustituidos como inhibidores de Janus Quinasas |
| KR20090129488A (ko) | 2007-03-22 | 2009-12-16 | 버텍스 파마슈티칼스 인코포레이티드 | 야누스 키나아제의 억제제로서 유용한 ｎ-헤테로사이클릭 화합물 |
| CL2008001709A1 (es) | 2007-06-13 | 2008-11-03 | Incyte Corp | Compuestos derivados de pirrolo [2,3-b]pirimidina, moduladores de quinasas jak; composicion farmaceutica; y uso en el tratamiento de enfermedades tales como cancer, psoriasis, artritis reumatoide, entre otras. |
| 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 |
| EP2262498A2 (en) * | 2008-03-10 | 2010-12-22 | Vertex Pharmceuticals Incorporated | Pyrimidines and pyridines useful as inhibitors of protein kinases |
| MY165582A (en) | 2008-03-11 | 2018-04-05 | Incyte Holdings Corp | Azetidine and cyclobutane derivatives as jak inhibitors |
| NZ590784A (en) * | 2008-07-23 | 2012-12-21 | Vertex Pharma | Pyrazolopyridine kinase inhibitors |
| NZ596479A (en) | 2009-05-22 | 2014-01-31 | 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 |
| BRPI1012108B8 (pt) | 2009-05-22 | 2021-05-25 | Incyte Corp | composto 3-[4-(7h-pirrolo[2,3-d]pirimidin-4-il)-1h-pirazol-1-il]octa no- ou heptano-nitrila, sua composição, seus usos e processo para preparar um sal de ácido fosfórico |
| GEP20207129B (en) | 2009-06-17 | 2020-07-10 | Vertex Pharma | Inhibitors of influenza viruses replication |
| 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 |
| EA021478B1 (ru) | 2009-10-09 | 2015-06-30 | Инсайт Корпорейшн | ГИДРОКСИЛЬНЫЕ, КЕТО И ГЛЮКУРОНИДНЫЕ ПРОИЗВОДНЫЕ 3-(4-(7Н-ПИРРОЛО[2,3-d]ПИРИМИДИН-4-ИЛ)-1Н-ПИРАЗОЛ-1-ИЛ)-3-ЦИКЛОПЕНТИЛПРОПАННИТРИЛА |
| EP2516434B1 (en) | 2009-12-23 | 2015-05-27 | Takeda Pharmaceutical Company Limited | Fused heteroaromatic pyrrolidinones as syk inhibitors |
| CA2792508C (en) | 2010-03-10 | 2018-01-16 | Incyte Corporation | Piperidin-4-yl azetidine derivatives as jak1 inhibitors |
| US8481541B2 (en) | 2010-03-22 | 2013-07-09 | Hoffmann-La Roche Inc. | Pyrrolopyrazine kinase inhibitors |
| EP2563125A4 (en) * | 2010-04-27 | 2013-10-02 | Merck Sharp & Dohme | AZAINDOLE AS JANUSKINASE HEMMER |
| MX2012013194A (es) | 2010-05-20 | 2013-01-22 | Hoffmann La Roche | Derivados pirrolopirazinas como inhibidores de cinasas tirocina-cinasa del baso (syk) y cinasa de janus (jak). |
| EA202091303A3 (ru) | 2010-05-21 | 2021-05-31 | Инсайт Холдингс Корпорейшн | Композиция ингибитора jak для местного применения |
| US9198911B2 (en) | 2010-11-02 | 2015-12-01 | The Trustees Of Columbia University In The City Of New York | Methods for treating hair loss disorders |
| CA2818542A1 (en) | 2010-11-19 | 2012-05-24 | Incyte Corporation | Cyclobutyl substituted pyrrolopyridine and pyrrolopyrimidine derivatives as jak inhibitors |
| ES2536415T3 (es) | 2010-11-19 | 2015-05-25 | Incyte Corporation | Pirrolopiridinas y pirrolopirimidinas sustituidas heterocíclicas como inhibidores de JAK |
| RU2013132681A (ru) | 2010-12-16 | 2015-01-27 | Вертекс Фармасьютикалз Инкорпорейтед | Ингибиторы репликации вирусов гриппа |
| JP2013545817A (ja) | 2010-12-16 | 2013-12-26 | バーテックス ファーマシューティカルズ インコーポレイテッド | インフルエンザウイルス複製阻害物質 |
| AU2011343647A1 (en) * | 2010-12-16 | 2013-05-02 | Vertex Pharmaceuticals Incorporated | Inhibitors of influenza viruses replication |
| DE102011009961A1 (de) * | 2011-02-01 | 2012-08-02 | Merck Patent Gmbh | 7-Azaindolderivate |
| WO2012112847A1 (en) | 2011-02-18 | 2012-08-23 | Novartis Pharma Ag | mTOR/JAK INHIBITOR COMBINATION THERAPY |
| AU2012232658B2 (en) | 2011-03-22 | 2016-06-09 | Advinus Therapeutics Limited | Substituted fused tricyclic compounds, compositions and medicinal applications thereof |
| JP2014515368A (ja) | 2011-05-26 | 2014-06-30 | 第一三共株式会社 | プロテインキナーゼ阻害剤としての複素環化合物 |
| US8691807B2 (en) | 2011-06-20 | 2014-04-08 | Incyte Corporation | Azetidinyl phenyl, pyridyl or pyrazinyl carboxamide derivatives as JAK inhibitors |
| WO2012177714A1 (en) | 2011-06-22 | 2012-12-27 | Takeda Pharmaceutical Company Limited | Substituted 6-aza-isoindolin-1-one derivatives |
| PL3141548T3 (pl) | 2011-07-05 | 2020-09-07 | Vertex Pharmaceuticals Incorporated | Sposoby i związki pośrednie do wytwarzania azaindoli |
| UA118010C2 (uk) * | 2011-08-01 | 2018-11-12 | Вертекс Фармасьютікалз Інкорпорейтед | Інгібітори реплікації вірусів грипу |
| WO2013023119A1 (en) | 2011-08-10 | 2013-02-14 | Novartis Pharma Ag | JAK P13K/mTOR COMBINATION THERAPY |
| 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 |
| EP2776036A1 (en) | 2011-11-07 | 2014-09-17 | Vertex Pharmaceuticals Incorporated | Methods for treating inflammatory diseases and pharmaceutical combinations useful therefor |
| US9089574B2 (en) | 2011-11-30 | 2015-07-28 | Emory University | Antiviral JAK inhibitors useful in treating or preventing retroviral and other viral infections |
| WO2013117649A1 (en) * | 2012-02-10 | 2013-08-15 | Galapagos Nv | Imidazo [4, 5 -c] pyridine derivatives useful for the treatment of degenerative and inflammatory diseases |
| UY34616A (es) * | 2012-02-10 | 2013-09-30 | Galapagos Nv | Nuevo compuesto útil para el tratamiento de enfermedades degenerativas e inflamatorias. |
| DK2830662T3 (da) * | 2012-03-29 | 2019-01-02 | Univ Columbia | Fremgangsmåder til behandlng af hårtabsforstyrrelser |
| US20130310340A1 (en) | 2012-05-16 | 2013-11-21 | Rigel Pharmaceuticals, Inc. | Method of treating muscular degradation |
| 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 |
| WO2013184985A1 (en) | 2012-06-08 | 2013-12-12 | Vertex Pharmaceuticals Incorporated | Inhibitors of influenza viruses replication |
| WO2014013014A1 (en) | 2012-07-18 | 2014-01-23 | Fundació Privada Centre De Regulació Genòmica (Crg) | Jak inhibitors for activation of epidermal stem cell populations |
| WO2014045305A1 (en) | 2012-09-21 | 2014-03-27 | Advinus Therapeutics Limited | Substituted fused tricyclic compounds, compositions and medicinal applications thereof |
| WO2014074471A1 (en) | 2012-11-06 | 2014-05-15 | Vertex Pharmaceuticals Incorporated | Methods for treating inflammatory diseases and pharmaceutical combinations useful therefor |
| KR102242077B1 (ko) | 2012-11-15 | 2021-04-20 | 인사이트 홀딩스 코포레이션 | 룩솔리티니브의 서방성 제형 |
| WO2014089280A1 (en) * | 2012-12-07 | 2014-06-12 | Calitor Sciences, Llc | Alkynyl compounds and methods of use |
| WO2014110259A1 (en) | 2013-01-09 | 2014-07-17 | Vertex Pharmaceuticals Incorporated | Solid forms of a jak inhibitor |
| US9695178B2 (en) * | 2013-01-15 | 2017-07-04 | Suzhou Kintor Pharmaceuticals, Inc. | 6-(2-pyridyl)-7,8-dihydro-5H-pyrido[4,3-D]pyrimidine analogs as hedgehog pathway signaling inhibitors and therapeutic applications thereof |
| TW201513861A (zh) * | 2013-01-17 | 2015-04-16 | Galapagos Nv | 用於治療退化性及發炎疾病之新穎化合物 |
| TWI736135B (zh) | 2013-03-01 | 2021-08-11 | 美商英塞特控股公司 | 吡唑并嘧啶衍生物治療PI3Kδ相關病症之用途 |
| EP3489239B1 (en) | 2013-03-06 | 2021-09-15 | Incyte Holdings Corporation | Processes and intermediates for making a jak inhibitor |
| EP2976338B1 (en) * | 2013-03-19 | 2018-01-03 | Merck Sharp & Dohme Corp. | N-(2-cyano heterocyclyl)pyrazolo pyridones as janus kinase inhibitors |
| WO2014201332A1 (en) * | 2013-06-14 | 2014-12-18 | Vertex Pharmaceuticals Incorporated | Pharmaceutical combinations useful for treating rheumatoid arthritis |
| MX376856B (es) | 2013-08-07 | 2025-03-07 | Incyte Holdings Corp | Formas de dosificacion de liberacion prolongada para un inhibidor de jak 1 (cinasa de janus 1). |
| KR20160045070A (ko) | 2013-08-22 | 2016-04-26 | 버텍스 파마슈티칼스 인코포레이티드 | 동위원소 풍부 아자인돌 |
| US9296727B2 (en) | 2013-10-07 | 2016-03-29 | Vertex Pharmaceuticals Incorporated | Methods of regioselective synthesis of 2,4-disubstituted pyrimidines |
| PT3068776T (pt) | 2013-11-13 | 2019-08-26 | Vertex Pharma | Inibidores da replicação de vírus da gripe |
| HUE038820T2 (hu) | 2013-11-13 | 2018-11-28 | Vertex Pharma | Eljárás influenzavírusok replikációjának inhibitorai elõállítására |
| ES2706306T3 (es) * | 2014-02-04 | 2019-03-28 | Taiho Pharmaceutical Co Ltd | Derivado de azaindol |
| WO2015184305A1 (en) | 2014-05-30 | 2015-12-03 | Incyte Corporation | TREATMENT OF CHRONIC NEUTROPHILIC LEUKEMIA (CNL) AND ATYPICAL CHRONIC MYELOID LEUKEMIA (aCML) BY INHIBITORS OF JAK1 |
| EA201790266A1 (ru) | 2014-08-08 | 2017-06-30 | Янссен Сайенсиз Айрлэнд Юси | Индолы для применения при инфекции, вызванной вирусом гриппа |
| NO2721710T3 (enExample) * | 2014-08-21 | 2018-03-31 | ||
| TWI679205B (zh) | 2014-09-02 | 2019-12-11 | 日商日本新藥股份有限公司 | 吡唑并噻唑化合物及醫藥 |
| MA40844A (fr) * | 2014-11-10 | 2017-09-20 | Glaxosmithkline Ip No 2 Ltd | Compositions pharmaceutiques à action prolongée pour l'hépatite c |
| JP6460382B2 (ja) * | 2014-11-28 | 2019-01-30 | 株式会社豊田自動織機 | 飽和ヘテロ環含有化合物、並びにこれを用いた二次電池用電極及び二次電池、結着剤、蛍光物質 |
| EP3294717B1 (en) | 2015-05-13 | 2020-07-29 | Vertex Pharmaceuticals Inc. | Methods of preparing inhibitors of influenza viruses replication |
| WO2016183120A1 (en) | 2015-05-13 | 2016-11-17 | Vertex Pharmaceuticals Incorporated | Inhibitors of influenza viruses replication |
| TWI712604B (zh) | 2016-03-01 | 2020-12-11 | 日商日本新藥股份有限公司 | 具jak抑制作用之化合物之結晶 |
| CN109071567B (zh) * | 2016-05-19 | 2021-03-23 | 四川大学 | 抗流感小分子化合物及其制备方法和用途 |
| EP3492468B1 (en) * | 2016-07-26 | 2022-02-23 | Suzhou Longbiotech Pharmaceuticals Co., Ltd. | Heterocyclic compound as jak inhibitor, and salts and therapeutic use thereof |
| WO2018041989A1 (en) | 2016-09-02 | 2018-03-08 | INSERM (Institut National de la Santé et de la Recherche Médicale) | Methods for diagnosing and treating refractory celiac disease type 2 |
| CA3059449A1 (en) | 2017-04-24 | 2018-11-01 | Cocrystal Pharma, Inc. | Pyrrolopyrimidine derivatives useful as inhibitors of influenza virus replication |
| 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 |
| MD3746429T2 (ro) | 2018-01-30 | 2022-08-31 | Incyte Corp | Procedee pentru prepararea de (1-(3-fluoro-2-(trifluorometil)izonicotinil)piperidin-4-onă) |
| TW201940483A (zh) | 2018-03-12 | 2019-10-16 | 美商艾伯維有限公司 | 酪胺酸激酶２介導的傳訊之抑制劑 |
| KR20260080448A (ko) | 2018-03-30 | 2026-06-02 | 인사이트 코포레이션 | Jak 억제제를 사용하는 화농성 한선염의 치료 |
| TWI821343B (zh) | 2018-07-27 | 2023-11-11 | 美商共結晶製藥公司 | 流感病毒複製之抑制劑 |
| EP3887355A1 (en) | 2018-11-26 | 2021-10-06 | Cocrystal Pharma, Inc. | Inhibitors of influenza virus replication |
| CA3129665A1 (en) | 2019-03-21 | 2020-09-24 | Onxeo | A dbait molecule in combination with kinase inhibitor for the treatment of cancer |
| WO2020201362A2 (en) | 2019-04-02 | 2020-10-08 | INSERM (Institut National de la Santé et de la Recherche Médicale) | Methods of predicting and preventing cancer in patients having premalignant lesions |
| WO2020212395A1 (en) | 2019-04-16 | 2020-10-22 | INSERM (Institut National de la Santé et de la Recherche Médicale) | Use of jak inhibitors for the treatment of painful conditions involving nav1.7 channels |
| KR102133595B1 (ko) | 2019-05-31 | 2020-07-13 | 에이치케이이노엔 주식회사 | 단백질 키나제 억제제로서의 헤테로고리 화합물 |
| KR102112336B1 (ko) | 2019-08-12 | 2020-05-18 | 에이치케이이노엔 주식회사 | 단백질 키나제 억제제로서의 헤테로고리 화합물 |
| CA3156007A1 (en) | 2019-09-27 | 2021-04-01 | Disc Medicine, Inc. | METHODS OF TREATING MYELOFIBROSE AND ASSOCIATED CONDITIONS |
| KR20220098759A (ko) | 2019-11-08 | 2022-07-12 | 인쎄름 (엥스띠뛰 나씨오날 드 라 쌍떼 에 드 라 흐쉐르슈 메디깔) | 키나제 억제제에 대해 내성을 획득한 암의 치료 방법 |
| WO2021148581A1 (en) | 2020-01-22 | 2021-07-29 | Onxeo | Novel dbait molecule and its use |
| US20230151034A1 (en) | 2020-03-17 | 2023-05-18 | Cocrystal Pharma, Inc. | Peptidomimetic n5-methyl-n2-(nonanoyl-l-leucyl)-l-glutaminate derivatives, triazaspiro[4.14]nonadecane derivatives and similar compounds as inhibitors of norovirus and coronavirus replication |
| WO2021206877A1 (en) | 2020-04-10 | 2021-10-14 | Cocrystal Pharma, Inc. | Inhibitors of norovirus and coronavirus replication |
| ES3075793T3 (en) | 2020-05-13 | 2026-08-07 | Disc Medicine Inc | Anti-hemojuvelin (hjv) antibodies for treating myelofibrosis |
| AU2021273014A1 (en) | 2020-05-13 | 2022-11-17 | AbbVie Deutschland GmbH & Co. KG | Anti-hemojuvelin (HJV) antibodies for treating anemia of chronic disease |
| US11833155B2 (en) | 2020-06-03 | 2023-12-05 | Incyte Corporation | Combination therapy for treatment of myeloproliferative neoplasms |
| US20250283174A1 (en) | 2022-05-16 | 2025-09-11 | Institut National de la Santé et de la Recherche Médicale | Methods for assessing the exhaustion of hematopoietic stem cells induced by chronic inflammation |
| CN120957983A (zh) * | 2023-04-17 | 2025-11-14 | 亚飞络思制药公司 | 取代的乙炔化合物衍生物及其药物用途 |
| WO2026093435A1 (en) | 2024-10-31 | 2026-05-07 | Institut National de la Santé et de la Recherche Médicale | Use of jak inhibitors for enhancing the potency of immunotherapy in the treament of cancer |
| WO2026134316A1 (ja) * | 2024-12-20 | 2026-06-25 | アステラス製薬株式会社 | ヘテロアリールアミド化合物 |
Family Cites Families (57)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| NZ221717A (en) | 1986-09-10 | 1990-08-28 | Sandoz Ltd | Azaindole and indolizine derivatives and pharmaceutical compositions |
| US5304121A (en) | 1990-12-28 | 1994-04-19 | Boston Scientific Corporation | Drug delivery system making use of a hydrogel polymer coating |
| FR2687402B1 (fr) * | 1992-02-14 | 1995-06-30 | Lipha | Nouveaux azaindoles, procedes de preparation et medicaments les contenant. |
| US5994341A (en) | 1993-07-19 | 1999-11-30 | Angiogenesis Technologies, Inc. | Anti-angiogenic Compositions and methods for the treatment of arthritis |
| US6075037A (en) | 1994-06-09 | 2000-06-13 | Smithkline Beecham Corporation | Endothelin receptor antagonists |
| US6099562A (en) | 1996-06-13 | 2000-08-08 | Schneider (Usa) Inc. | Drug coating with topcoat |
| GB9721437D0 (en) | 1997-10-10 | 1997-12-10 | Glaxo Group Ltd | Heteroaromatic compounds and their use in medicine |
| FR2784375B1 (fr) * | 1998-10-12 | 2000-11-24 | Adir | Nouveaux derives cycliques a chaine cycloalkylenique, leur procede de preparation et les compositions pharmaceutiques qui les contiennent |
| US6265403B1 (en) | 1999-01-20 | 2001-07-24 | Merck & Co., Inc. | Angiogenesis inhibitors |
| US20030153560A1 (en) | 1999-04-23 | 2003-08-14 | Salituro Francesco G. | Inhibitors of c-Jun N-terminal kinases (JNK) |
| DE60027431T2 (de) | 1999-07-02 | 2007-07-12 | Stuart A. Rancho Santa Fe Lipton | Verwendung von p38 MAPK Inhibitoren in der Behandlung von Augenkrankheiten |
| CA2396693A1 (en) | 1999-12-28 | 2001-07-05 | Stephen T. Wrobleski | Cytokine, especially tnf-alpha, inhibitors |
| KR20030024659A (ko) | 2000-02-17 | 2003-03-26 | 암겐 인코포레이티드 | 키나제 억제제 |
| AU2001290912A1 (en) | 2000-09-15 | 2002-03-26 | Vertex Pharmaceuticals Incorporated | Pyrazole compounds useful as protein kinase inhibitors |
| ATE497603T1 (de) * | 2001-03-02 | 2011-02-15 | Gpc Biotech Ag | Drei-hybrid-assaysystem |
| US7081454B2 (en) | 2001-03-28 | 2006-07-25 | Bristol-Myers Squibb Co. | Tyrosine kinase inhibitors |
| CA2450769A1 (en) | 2001-06-15 | 2002-12-27 | Vertex Pharmaceuticals Incorporated | 5-(2-aminopyrimidin-4-yl) benzisoxazoles as protein kinase inhibitors |
| GB0115109D0 (en) | 2001-06-21 | 2001-08-15 | Aventis Pharma Ltd | Chemical compounds |
| US20040236110A1 (en) | 2001-09-26 | 2004-11-25 | Ladouceur Gaetan H | Substituted 3-pyridyl indoles and indazoles as c17,20 lyase inhibitors |
| TW200306819A (en) | 2002-01-25 | 2003-12-01 | Vertex Pharma | Indazole compounds useful as protein kinase inhibitors |
| AU2003216660A1 (en) | 2002-04-26 | 2003-11-10 | Pfizer Products Inc. | N-substituted-heteroaryloxy-aryl-spiro-pyrimidine-2,4,6-trione metalloproteinase inhibitors |
| EP1506189A1 (en) | 2002-04-26 | 2005-02-16 | Vertex Pharmaceuticals Incorporated | Pyrrole derivatives as inhibitors of erk2 and uses thereof |
| CN1656079A (zh) | 2002-05-31 | 2005-08-17 | 卫材株式会社 | 吡唑化合物和含有该化合物的药物组合物 |
| UA78999C2 (en) | 2002-06-04 | 2007-05-10 | Wyeth Corp | 1-(aminoalkyl)-3-sulfonylazaindoles as ligands of 5-hydroxytryptamine-6 |
| MXPA05001367A (es) | 2002-08-02 | 2005-04-28 | Vertex Pharma | Composiciones de pirazol utiles como inhibidores de gsk-3. |
| SE0202463D0 (sv) | 2002-08-14 | 2002-08-14 | Astrazeneca Ab | Novel compounds |
| US7262200B2 (en) | 2002-10-25 | 2007-08-28 | Vertex Pharmaceuticals Incorporated | Indazolinone compositions useful as kinase inhibitors |
| US7432375B2 (en) | 2003-03-06 | 2008-10-07 | Eisai R & D Management Co., Ltd. | JNK inhibitors |
| US7375228B2 (en) | 2003-03-17 | 2008-05-20 | Takeda San Diego, Inc. | Histone deacetylase inhibitors |
| GB0308466D0 (en) | 2003-04-11 | 2003-05-21 | Novartis Ag | Organic compounds |
| TWI339206B (en) * | 2003-09-04 | 2011-03-21 | Vertex Pharma | Compositions useful as inhibitors of protein kinases |
| WO2005044181A2 (en) | 2003-09-09 | 2005-05-19 | Temple University-Of The Commonwealth System Of Higher Education | Protection of tissues and cells from cytotoxic effects of ionizing radiation by abl inhibitors |
| CN1897950A (zh) | 2003-10-14 | 2007-01-17 | 惠氏公司 | 稠合芳基和杂芳基衍生物及其使用方法 |
| JP5138938B2 (ja) | 2003-12-19 | 2013-02-06 | プレキシコン インコーポレーテッド | Ｒｅｔ調節剤の開発のための化合物および方法 |
| ES2364340T3 (es) | 2004-03-30 | 2011-08-31 | Vertex Pharmaceuticals Incorporated | Azaindoles útiles como inhibidores de jak y otras proteína quinasas. |
| US7514448B2 (en) * | 2004-04-02 | 2009-04-07 | Vertex Pharmaceuticals Incorporated | Azaindoles useful as inhibitors of rock and other protein kinases |
| TW200616632A (en) | 2004-06-17 | 2006-06-01 | Plexxikon Inc | Compounds modulating c-kit activity and uses therefor |
| US20060122213A1 (en) * | 2004-06-30 | 2006-06-08 | Francoise Pierard | Azaindoles useful as inhibitors of protein kinases |
| NZ553267A (en) | 2004-07-27 | 2010-09-30 | Sgx Pharmaceuticals Inc | Pyrrolo-pyridine kinase modulators |
| GB0420719D0 (en) | 2004-09-17 | 2004-10-20 | Addex Pharmaceuticals Sa | Novel allosteric modulators |
| WO2006038001A1 (en) | 2004-10-06 | 2006-04-13 | Celltech R & D Limited | Aminopyrimidine derivatives as jnk inhibitors |
| WO2006050076A1 (en) | 2004-10-29 | 2006-05-11 | Janssen Pharmaceutica, N.V. | Pyrimidinyl substituted fused-pyrrolyl compounds useful in treating kinase disorders |
| AU2005309566A1 (en) | 2004-11-22 | 2006-06-01 | Vertex Pharmaceuticals Incorporated | Bicyclic inhibitors or Rho kinase |
| MX2007007330A (es) | 2004-12-16 | 2007-10-04 | Vertex Pharma | Piridonas de utilidad como inhibidores de quinasas . |
| US8633205B2 (en) * | 2005-02-03 | 2014-01-21 | Vertex Pharmaceuticals Incorporated | Substituted pyrrolo[2,3-d]pyrimidines as inhibitors of protein kinases |
| AU2006247322A1 (en) | 2005-05-16 | 2006-11-23 | Irm Llc | Pyrrolopyridine derivatives as protein kinase inhibitors |
| JP2008545660A (ja) | 2005-05-20 | 2008-12-18 | バーテックス ファーマシューティカルズ インコーポレイテッド | プロテインキナーゼ阻害剤として有用なピロロピリジン化合物 |
| MY153898A (en) | 2005-06-22 | 2015-04-15 | Plexxikon Inc | Compounds and methods for kinase modulation, and indications therefor |
| CN101801971A (zh) * | 2005-09-30 | 2010-08-11 | 沃泰克斯药物股份有限公司 | 可用作janus激酶抑制剂的脱氮嘌呤 |
| NZ592968A (en) * | 2006-01-17 | 2012-08-31 | Vertex Pharma | Azaindoles substituted with either triazine or pyrimidine useful as inhibitors of janus kinases consisting of JAK1, JAK2, JAK3, and TYK2 |
| WO2007095223A2 (en) | 2006-02-14 | 2007-08-23 | Vertex Pharmaceuticals Incorporated | Pyrrolo(3,2-c) pyridines useful as inhibitors of protein kinases |
| JP2009532475A (ja) | 2006-04-05 | 2009-09-10 | バーテックス ファーマシューティカルズ インコーポレイテッド | ヤヌスキナーゼの阻害剤として有用なデアザプリン |
| US8129387B2 (en) | 2006-12-14 | 2012-03-06 | Vertex Pharmaceuticals Incorporated | Substituted 5,6-dihydroimidazo[1,5-F]pteridines useful as protein kinase inhibitors |
| US8541437B2 (en) | 2007-04-05 | 2013-09-24 | Alla Chem, Llc | Substituted 2,3,4,5-tetrahydro-1H-pyrido[4,3-b]indoles, methods for the production and use thereof |
| US8173635B2 (en) | 2007-11-02 | 2012-05-08 | Vertex Pharmaceuticals Incorporated | Kinase inhibitors |
| EP2262498A2 (en) | 2008-03-10 | 2010-12-22 | Vertex Pharmceuticals Incorporated | Pyrimidines and pyridines useful as inhibitors of protein kinases |
| EP2776036A1 (en) | 2011-11-07 | 2014-09-17 | Vertex Pharmaceuticals Incorporated | Methods for treating inflammatory diseases and pharmaceutical combinations useful therefor |
-
2007
- 2007-01-17 NZ NZ59296807A patent/NZ592968A/xx not_active IP Right Cessation
- 2007-01-17 TW TW101137542A patent/TWI423976B/zh not_active IP Right Cessation
- 2007-01-17 TW TW101137037A patent/TWI424999B/zh not_active IP Right Cessation
- 2007-01-17 TW TW96101771A patent/TWI405761B/zh not_active IP Right Cessation
- 2007-01-17 CA CA 2636189 patent/CA2636189A1/en not_active Abandoned
- 2007-01-17 CN CN2011104033161A patent/CN102532134A/zh active Pending
- 2007-01-17 EP EP20120176813 patent/EP2537849A3/en not_active Withdrawn
- 2007-01-17 CN CN201510004860.7A patent/CN104650077A/zh active Pending
- 2007-01-17 EP EP07718337.4A patent/EP1973911B1/en active Active
- 2007-01-17 KR KR1020137005929A patent/KR20130041313A/ko not_active Withdrawn
- 2007-01-17 NZ NZ569899A patent/NZ569899A/en not_active IP Right Cessation
- 2007-01-17 UA UAA200810409A patent/UA95940C2/uk unknown
- 2007-01-17 NZ NZ60168707A patent/NZ601687A/en not_active IP Right Cessation
- 2007-01-17 CN CN2011103519191A patent/CN102532133A/zh active Pending
- 2007-01-17 JP JP2008551353A patent/JP5591471B2/ja not_active Expired - Fee Related
- 2007-01-17 BR BRPI0722364-1A patent/BRPI0722364A2/pt not_active IP Right Cessation
- 2007-01-17 KR KR1020087017472A patent/KR101409727B1/ko not_active Expired - Fee Related
- 2007-01-17 AU AU2007207533A patent/AU2007207533B8/en not_active Ceased
- 2007-01-17 AR ARP070100199 patent/AR060316A1/es unknown
- 2007-01-17 KR KR1020127014597A patent/KR101235103B1/ko not_active Expired - Fee Related
- 2007-01-17 WO PCT/US2007/001225 patent/WO2007084557A2/en not_active Ceased
- 2007-01-17 TW TW102147300A patent/TW201412738A/zh unknown
- 2007-01-17 RU RU2008133613/04A patent/RU2453548C2/ru not_active IP Right Cessation
- 2007-01-17 US US11/654,375 patent/US7767816B2/en not_active Expired - Fee Related
- 2007-01-17 BR BRPI0706537-0A patent/BRPI0706537A2/pt not_active IP Right Cessation
- 2007-01-17 EP EP20120176810 patent/EP2559694A3/en not_active Withdrawn
-
2008
- 2008-06-03 IL IL191902A patent/IL191902A0/en unknown
- 2008-06-10 ZA ZA2008/05053A patent/ZA200805053B/en unknown
- 2008-07-21 CL CL2008002140A patent/CL2008002140A1/es unknown
- 2008-08-13 NO NO20083501A patent/NO20083501L/no not_active Application Discontinuation
-
2009
- 2009-04-30 HK HK15111605.7A patent/HK1210780A1/xx unknown
- 2009-06-12 ZA ZA2009/04147A patent/ZA200904147B/en unknown
-
2010
- 2010-05-07 US US12/775,885 patent/US8163917B2/en not_active Expired - Fee Related
-
2011
- 2011-12-14 RU RU2011151085/02A patent/RU2011151085A/ru not_active Application Discontinuation
-
2012
- 2012-03-01 US US13/409,702 patent/US8450489B2/en not_active Expired - Fee Related
- 2012-10-11 JP JP2012226368A patent/JP2013010793A/ja not_active Ceased
- 2012-10-11 JP JP2012226367A patent/JP5728454B2/ja not_active Expired - Fee Related
-
2013
- 2013-04-25 US US13/870,173 patent/US8822681B2/en not_active Expired - Fee Related
-
2014
- 2014-07-24 US US14/339,514 patent/US9120790B2/en not_active Expired - Fee Related
- 2014-08-20 JP JP2014167160A patent/JP2014210823A/ja active Pending
-
2015
- 2015-07-29 US US14/812,158 patent/US20160008359A1/en not_active Abandoned
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| JP2013010792A5 (enExample) | ||
| AU2007282080B2 (en) | Isoform-selective HDAC inhibitors | |
| JP2018515495A5 (enExample) | ||
| JP2017537940A5 (enExample) | ||
| RU2018105549A (ru) | Производные бензодиазепина как ингибиторы rsv | |
| EA201650029A1 (ru) | Пиразолопиридины и пиразолопиримидины | |
| JP2008545660A5 (enExample) | ||
| JP2013500314A5 (enExample) | ||
| RU2014141579A (ru) | Гетероциклические соединения в качестве ингибиторов бета-лактамаз | |
| JP2015537020A5 (enExample) | ||
| RU2015107803A (ru) | Производные дигидроксипиримидинкарбоновой кислоты и их применение в лечении, облегчении или предотвращении вирусного заболевания | |
| JP2016518305A5 (enExample) | ||
| JP2016528180A5 (enExample) | ||
| NO20091858L (no) | Hydrobenzamid derivater som inhibitorer av HSP90 | |
| RU2019141734A (ru) | Терапевтические соединения и композиции и способы их применения | |
| JP2020520957A5 (enExample) | ||
| JOP20240217A1 (ar) | مشتقات الكوينولين كمُعدِّلات للعضو x2 لمستقبل بروتين g مرتبط بـ mas ومنتجات ذات صلة | |
| RU2017117559A (ru) | Бензопроизводные с шестичленным кольцом в качестве ингибитора dpp-4 и их применение | |
| JP2019530674A5 (enExample) | ||
| JP2016508145A5 (enExample) | ||
| JP2022536160A5 (enExample) | ||
| JP2018527324A5 (enExample) | ||
| JP2011519845A5 (enExample) | ||
| TW201641492A (zh) | 經取代1,2,3-三唑、其用途、以及包含其之醫藥組成物 | |
| RU2010148420A (ru) | Производные аминопиридина |