JP2013010793A5 - - Google Patents
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- 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
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- 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) | KR101235103B1 (enExample) |
| CN (3) | CN102532133A (enExample) |
| AR (1) | AR060316A1 (enExample) |
| AU (1) | AU2007207533B8 (enExample) |
| BR (2) | BRPI0706537A2 (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 (101)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CA2560454C (en) | 2004-03-30 | 2013-05-21 | Vertex Pharmaceuticals Incorporated | Azaindoles useful as inhibitors of jak and other protein kinases |
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| EP2270014A1 (en) | 2005-09-22 | 2011-01-05 | Incyte Corporation | Azepine inhibitors of janus kinases |
| DK3184526T3 (en) | 2005-12-13 | 2019-01-14 | Incyte Holdings Corp | PYRROLO [2,3-D] PYRIMIDINE DERIVATIVES AS A JANUS-KINASE INHIBITOR |
| EP2537849A3 (en) * | 2006-01-17 | 2013-04-03 | Vertex Pharmaceuticals, Inc. | Azaindoles useful as inhibitors of janus kinases |
| RU2008143361A (ru) * | 2006-04-05 | 2010-05-10 | Вертекс Фармасьютикалз Инкорпорейтед (Us) | Деазапурины в качестве ингибиторов янус-киназ |
| 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 |
| NZ577798A (en) * | 2006-12-21 | 2012-04-27 | Vertex Pharma | 5-cyano-4- (pyrrolo [2, 3b] pyridine-3-yl) -pyrimidine derivatives useful as protein kinase inhibitors |
| US8513270B2 (en) | 2006-12-22 | 2013-08-20 | Incyte Corporation | Substituted heterocycles as Janus kinase inhibitors |
| AU2008228768A1 (en) * | 2007-03-22 | 2008-09-25 | Vertex Pharmaceuticals Incorporated | N-heterocyclic compounds useful as inhibitors of Janus Kinases |
| 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 |
| 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. |
| WO2009145814A2 (en) * | 2008-03-10 | 2009-12-03 | Vertex Pharmaceuticals Incorporated | Pyrimidines and pyridines useful as inhibitors of protein kinases |
| ES2602577T3 (es) | 2008-03-11 | 2017-02-21 | Incyte Holdings Corporation | Derivados de azetidina y ciclobutano como inhibidores de JAK |
| JP2011529062A (ja) * | 2008-07-23 | 2011-12-01 | 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 | ピラゾロピリジンキナーゼ阻害剤 |
| WO2010135621A1 (en) | 2009-05-22 | 2010-11-25 | Incyte Corporation | 3-[4-(7h-pyrrolo[2,3-d]pyrimidin-4-yl)-1h-pyrazol-1-yl]octane- or heptane-nitrile as jak inhibitors |
| ES2487542T3 (es) | 2009-05-22 | 2014-08-21 | Incyte Corporation | Derivados de N-(hetero)aril-pirrolidina de pirazol-4-il-pirrolo[2,3-d]pirimidinas y pirrol-3-il-pirrolo[2,3-d]pirimidinas como inhibidores de cinasas Janus |
| GEP20207129B (en) * | 2009-06-17 | 2020-07-10 | Vertex Pharma | Inhibitors of influenza viruses replication |
| WO2011028685A1 (en) | 2009-09-01 | 2011-03-10 | Incyte Corporation | Heterocyclic derivatives of pyrazol-4-yl-pyrrolo[2,3-d]pyrimidines as janus kinase inhibitors |
| CA2777114C (en) | 2009-10-09 | 2018-10-23 | Incyte Corporation | Hydroxyl, keto, and glucuronide derivatives of 3-(4-(7h-pyrrolo[2,3-d]pyrimidin-4-yl)-1h-pyrazol-1-yl)-3-cyclopentylpropanenitrile |
| SG181857A1 (en) | 2009-12-23 | 2012-07-30 | Takeda Pharmaceutical | Fused heteroaromatic pyrrolidinones as syk inhibitors |
| SMT201800137T1 (it) | 2010-03-10 | 2018-07-17 | Incyte Holdings Corp | Derivati di piperidin-4-il azetidina come inibitori di jak1 |
| US8481541B2 (en) | 2010-03-22 | 2013-07-09 | Hoffmann-La Roche Inc. | Pyrrolopyrazine kinase inhibitors |
| WO2011137022A1 (en) * | 2010-04-27 | 2011-11-03 | Merck Sharp & Dohme Corp. | Azaindoles as janus kinase inhibitors |
| CA2798970A1 (en) | 2010-05-20 | 2011-11-24 | F. Hoffmann-La Roche Ag | Pyrrolopyrazine derivatives as syk and jak inhibitors |
| PH12012502296B1 (en) | 2010-05-21 | 2017-10-06 | Incyte Holdings Corp | Topical formulation for a jak inhibitor |
| 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 |
| ES2536415T3 (es) | 2010-11-19 | 2015-05-25 | Incyte Corporation | Pirrolopiridinas y pirrolopirimidinas sustituidas heterocíclicas como inhibidores de JAK |
| SG190839A1 (en) | 2010-11-19 | 2013-07-31 | Incyte Corp | Cyclobutyl substituted pyrrolopyridine and pyrrolopyrimidine derivatives as jak inhibitors |
| CN103492381A (zh) | 2010-12-16 | 2014-01-01 | 沃泰克斯药物股份有限公司 | 流感病毒复制的抑制剂 |
| WO2012083122A1 (en) | 2010-12-16 | 2012-06-21 | Vertex Pharmaceutical Incorporated | Inhibitors of influenza viruses replication |
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| DE102011009961A1 (de) | 2011-02-01 | 2012-08-02 | Merck Patent Gmbh | 7-Azaindolderivate |
| ES2547916T3 (es) | 2011-02-18 | 2015-10-09 | Novartis Pharma Ag | Terapia de combinación de inhibidores de mTOR/JAK |
| EP2688890B1 (en) | 2011-03-22 | 2017-08-30 | Advinus Therapeutics Limited | Substituted fused tricyclic compounds, compositions and medicinal applications thereof |
| WO2012160464A1 (en) | 2011-05-26 | 2012-11-29 | Daiichi Sankyo Company, Limited | Heterocyclic compounds as protein kinase inhibitors |
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| US9056873B2 (en) | 2011-06-22 | 2015-06-16 | Takeda Pharmaceutical Company Limited | Substituted 6-aza-isoindolin-1-one derivatives |
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| 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 |
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| UY34615A (es) * | 2012-02-10 | 2013-09-30 | Galapagos Nv | Nuevos compuestos útiles para el tratamiento de enfermedades degenerativas e inflamatorias. |
| CN104334191A (zh) * | 2012-03-29 | 2015-02-04 | 纽约市哥伦比亚大学托管会 | 治疗毛发脱落疾病的方法 |
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| 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 |
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