JP2007531760A5 - - Google Patents
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- Publication number
- JP2007531760A5 JP2007531760A5 JP2007506535A JP2007506535A JP2007531760A5 JP 2007531760 A5 JP2007531760 A5 JP 2007531760A5 JP 2007506535 A JP2007506535 A JP 2007506535A JP 2007506535 A JP2007506535 A JP 2007506535A JP 2007531760 A5 JP2007531760 A5 JP 2007531760A5
- Authority
- JP
- Japan
- Prior art keywords
- heteroatoms
- optionally substituted
- compound
- independently
- nitrogen
- 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
- IJGRMHOSHXDMSA-UHFFFAOYSA-N Atomic nitrogen Chemical compound N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims 75
- 125000005842 heteroatom Chemical group 0.000 claims 71
- 150000001875 compounds Chemical class 0.000 claims 62
- 125000002950 monocyclic group Chemical group 0.000 claims 49
- 229910052757 nitrogen Inorganic materials 0.000 claims 42
- 229920006395 saturated elastomer Polymers 0.000 claims 41
- NINIDFKCEFEMDL-UHFFFAOYSA-N Sulfur Chemical compound [S] NINIDFKCEFEMDL-UHFFFAOYSA-N 0.000 claims 40
- QVGXLLKOCUKJST-UHFFFAOYSA-N atomic oxygen Chemical compound [O] QVGXLLKOCUKJST-UHFFFAOYSA-N 0.000 claims 40
- 229910052760 oxygen Inorganic materials 0.000 claims 40
- 239000001301 oxygen Substances 0.000 claims 40
- 229910052717 sulfur Inorganic materials 0.000 claims 40
- 239000011593 sulfur Substances 0.000 claims 40
- 229910052739 hydrogen Inorganic materials 0.000 claims 38
- 239000001257 hydrogen Substances 0.000 claims 38
- 125000004093 cyano group Chemical group *C#N 0.000 claims 27
- 229910052736 halogen Inorganic materials 0.000 claims 20
- 150000002367 halogens Chemical class 0.000 claims 20
- 125000002619 bicyclic group Chemical group 0.000 claims 19
- 150000002431 hydrogen Chemical class 0.000 claims 19
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 18
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 12
- 125000004429 atom Chemical group 0.000 claims 11
- 125000000217 alkyl group Chemical group 0.000 claims 10
- 239000003814 drug Substances 0.000 claims 10
- 125000001309 chloro group Chemical group Cl* 0.000 claims 9
- 125000001246 bromo group Chemical group Br* 0.000 claims 8
- 125000000325 methylidene group Chemical group [H]C([H])=* 0.000 claims 7
- 125000001160 methoxycarbonyl group Chemical group [H]C([H])([H])OC(*)=O 0.000 claims 6
- 229940124597 therapeutic agent Drugs 0.000 claims 6
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 claims 5
- 125000004122 cyclic group Chemical group 0.000 claims 5
- 239000000203 mixture Substances 0.000 claims 5
- QJGQUHMNIGDVPM-UHFFFAOYSA-N nitrogen group Chemical group [N] QJGQUHMNIGDVPM-UHFFFAOYSA-N 0.000 claims 5
- -1 2-substituted phenyl Chemical group 0.000 claims 4
- 125000001931 aliphatic group Chemical group 0.000 claims 4
- 125000001797 benzyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])* 0.000 claims 4
- 229940079593 drug Drugs 0.000 claims 4
- 125000001449 isopropyl group Chemical group [H]C([H])([H])C([H])(*)C([H])([H])[H] 0.000 claims 3
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 claims 2
- 239000002671 adjuvant Substances 0.000 claims 2
- 125000002618 bicyclic heterocycle group Chemical group 0.000 claims 2
- 239000003937 drug carrier Substances 0.000 claims 2
- 201000006417 multiple sclerosis Diseases 0.000 claims 2
- 125000004433 nitrogen atom Chemical group N* 0.000 claims 2
- ILMRJRBKQSSXGY-UHFFFAOYSA-N tert-butyl(dimethyl)silicon Chemical group C[Si](C)C(C)(C)C ILMRJRBKQSSXGY-UHFFFAOYSA-N 0.000 claims 2
- 125000000025 triisopropylsilyl group Chemical group C(C)(C)[Si](C(C)C)(C(C)C)* 0.000 claims 2
- 239000003981 vehicle Substances 0.000 claims 2
- 208000024827 Alzheimer disease Diseases 0.000 claims 1
- 102000003989 Aurora kinases Human genes 0.000 claims 1
- 108090000433 Aurora kinases Proteins 0.000 claims 1
- 208000019838 Blood disease Diseases 0.000 claims 1
- 208000020084 Bone disease Diseases 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
- 208000018737 Parkinson disease Diseases 0.000 claims 1
- 102100025387 Tyrosine-protein kinase JAK3 Human genes 0.000 claims 1
- 101710112792 Tyrosine-protein kinase JAK3 Proteins 0.000 claims 1
- 229940124599 anti-inflammatory drug Drugs 0.000 claims 1
- 230000001028 anti-proliverative effect Effects 0.000 claims 1
- 239000002246 antineoplastic agent Substances 0.000 claims 1
- 125000003118 aryl group Chemical group 0.000 claims 1
- 208000006673 asthma Diseases 0.000 claims 1
- 239000012472 biological sample Substances 0.000 claims 1
- 229910052799 carbon Inorganic materials 0.000 claims 1
- 125000004432 carbon atom Chemical group C* 0.000 claims 1
- 239000002327 cardiovascular agent Substances 0.000 claims 1
- 229940125692 cardiovascular agent Drugs 0.000 claims 1
- 238000006243 chemical reaction Methods 0.000 claims 1
- 239000003795 chemical substances by application Substances 0.000 claims 1
- 229940127089 cytotoxic agent Drugs 0.000 claims 1
- 230000001066 destructive effect Effects 0.000 claims 1
- 230000000694 effects Effects 0.000 claims 1
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims 1
- 125000002541 furyl group Chemical group 0.000 claims 1
- 208000014951 hematologic disease Diseases 0.000 claims 1
- 208000018706 hematopoietic system disease Diseases 0.000 claims 1
- 125000001072 heteroaryl group Chemical group 0.000 claims 1
- 125000000623 heterocyclic group Chemical group 0.000 claims 1
- 125000004435 hydrogen atom Chemical group [H]* 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
- 230000002401 inhibitory effect Effects 0.000 claims 1
- 208000019423 liver disease Diseases 0.000 claims 1
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 1
- 125000004108 n-butyl group Chemical group [H]C([H])([H])C([H])([H])C([H])([H])C([H])([H])* 0.000 claims 1
- 125000004123 n-propyl group Chemical group [H]C([H])([H])C([H])([H])C([H])([H])* 0.000 claims 1
- 239000003900 neurotrophic factor Substances 0.000 claims 1
- 125000001715 oxadiazolyl group Chemical group 0.000 claims 1
- 125000002971 oxazolyl group Chemical group 0.000 claims 1
- 239000008194 pharmaceutical composition Substances 0.000 claims 1
- 125000003373 pyrazinyl group Chemical group 0.000 claims 1
- 125000003226 pyrazolyl group Chemical group 0.000 claims 1
- 125000004076 pyridyl group Chemical group 0.000 claims 1
- 125000000714 pyrimidinyl group Chemical group 0.000 claims 1
- 125000000168 pyrrolyl group Chemical group 0.000 claims 1
- 239000011435 rock Substances 0.000 claims 1
- 150000003839 salts Chemical class 0.000 claims 1
- 201000000980 schizophrenia Diseases 0.000 claims 1
- 229940126585 therapeutic drug Drugs 0.000 claims 1
- 125000001113 thiadiazolyl group Chemical group 0.000 claims 1
- 125000000335 thiazolyl group Chemical group 0.000 claims 1
- 125000001544 thienyl group Chemical group 0.000 claims 1
- 125000001425 triazolyl group Chemical group 0.000 claims 1
- XEKOWRVHYACXOJ-UHFFFAOYSA-N Ethyl acetate Chemical compound CCOC(C)=O XEKOWRVHYACXOJ-UHFFFAOYSA-N 0.000 description 5
- YYROPELSRYBVMQ-UHFFFAOYSA-N 4-toluenesulfonyl chloride Chemical compound CC1=CC=C(S(Cl)(=O)=O)C=C1 YYROPELSRYBVMQ-UHFFFAOYSA-N 0.000 description 2
- 235000019439 ethyl acetate Nutrition 0.000 description 2
- VLKZOEOYAKHREP-UHFFFAOYSA-N n-Hexane Chemical class CCCCCC VLKZOEOYAKHREP-UHFFFAOYSA-N 0.000 description 2
- 125000003349 3-pyridyl group Chemical group N1=C([H])C([*])=C([H])C([H])=C1[H] 0.000 description 1
- 238000003818 flash chromatography Methods 0.000 description 1
- REPVNSJSTLRQEQ-UHFFFAOYSA-N n,n-dimethylacetamide;n,n-dimethylformamide Chemical compound CN(C)C=O.CN(C)C(C)=O REPVNSJSTLRQEQ-UHFFFAOYSA-N 0.000 description 1
- 239000012044 organic layer Substances 0.000 description 1
- 239000011541 reaction mixture Substances 0.000 description 1
- 239000007787 solid Substances 0.000 description 1
- 238000003756 stirring Methods 0.000 description 1
- 239000000725 suspension Substances 0.000 description 1
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 description 1
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US55750304P | 2004-03-30 | 2004-03-30 | |
| US60/557,503 | 2004-03-30 | ||
| US62559904P | 2004-11-05 | 2004-11-05 | |
| US60/625,599 | 2004-11-05 | ||
| PCT/US2005/010846 WO2005095400A1 (en) | 2004-03-30 | 2005-03-30 | Azaindoles useful as inhibitors of jak and other protein kinases |
Related Child Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2008060340A Division JP5042888B2 (ja) | 2004-03-30 | 2008-03-10 | Ｊａｋおよび他のプロテインキナーゼの阻害剤として有用なアザインドール |
| JP2011264040A Division JP5566992B2 (ja) | 2004-03-30 | 2011-12-01 | Ｊａｋおよび他のプロテインキナーゼの阻害剤として有用なアザインドール |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2007531760A JP2007531760A (ja) | 2007-11-08 |
| JP2007531760A5 true JP2007531760A5 (enExample) | 2012-01-26 |
| JP4937112B2 JP4937112B2 (ja) | 2012-05-23 |
Family
ID=34971569
Family Applications (5)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2007506535A Expired - Fee Related JP4937112B2 (ja) | 2004-03-30 | 2005-03-30 | Ｊａｋおよび他のプロテインキナーゼの阻害剤として有用なアザインドール |
| JP2008060340A Expired - Fee Related JP5042888B2 (ja) | 2004-03-30 | 2008-03-10 | Ｊａｋおよび他のプロテインキナーゼの阻害剤として有用なアザインドール |
| JP2011264040A Expired - Fee Related JP5566992B2 (ja) | 2004-03-30 | 2011-12-01 | Ｊａｋおよび他のプロテインキナーゼの阻害剤として有用なアザインドール |
| JP2013183669A Withdrawn JP2013249315A (ja) | 2004-03-30 | 2013-09-05 | Ｊａｋおよび他のプロテインキナーゼの阻害剤として有用なアザインドール |
| JP2015051664A Withdrawn JP2015113347A (ja) | 2004-03-30 | 2015-03-16 | Ｊａｋおよび他のプロテインキナーゼの阻害剤として有用なアザインドール |
Family Applications After (4)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2008060340A Expired - Fee Related JP5042888B2 (ja) | 2004-03-30 | 2008-03-10 | Ｊａｋおよび他のプロテインキナーゼの阻害剤として有用なアザインドール |
| JP2011264040A Expired - Fee Related JP5566992B2 (ja) | 2004-03-30 | 2011-12-01 | Ｊａｋおよび他のプロテインキナーゼの阻害剤として有用なアザインドール |
| JP2013183669A Withdrawn JP2013249315A (ja) | 2004-03-30 | 2013-09-05 | Ｊａｋおよび他のプロテインキナーゼの阻害剤として有用なアザインドール |
| JP2015051664A Withdrawn JP2015113347A (ja) | 2004-03-30 | 2015-03-16 | Ｊａｋおよび他のプロテインキナーゼの阻害剤として有用なアザインドール |
Country Status (26)
| Country | Link |
|---|---|
| US (6) | US7507826B2 (enExample) |
| EP (4) | EP2332940B1 (enExample) |
| JP (5) | JP4937112B2 (enExample) |
| KR (3) | KR101298951B1 (enExample) |
| CN (3) | CN103554104A (enExample) |
| AR (2) | AR048454A1 (enExample) |
| AT (1) | ATE508129T1 (enExample) |
| AU (3) | AU2005228904C1 (enExample) |
| BR (1) | BRPI0509369B1 (enExample) |
| CA (1) | CA2560454C (enExample) |
| CY (2) | CY1111716T1 (enExample) |
| DE (1) | DE602005027825D1 (enExample) |
| DK (2) | DK1730146T3 (enExample) |
| ES (2) | ES2364340T3 (enExample) |
| HR (1) | HRP20110566T8 (enExample) |
| IL (2) | IL177807A (enExample) |
| MX (1) | MXPA06011327A (enExample) |
| NO (2) | NO340403B1 (enExample) |
| NZ (2) | NZ584499A (enExample) |
| PL (2) | PL1730146T3 (enExample) |
| PT (2) | PT1730146E (enExample) |
| RS (1) | RS51830B (enExample) |
| RU (2) | RU2403252C2 (enExample) |
| SI (1) | SI1730146T1 (enExample) |
| TW (3) | TWI471133B (enExample) |
| WO (1) | WO2005095400A1 (enExample) |
Families Citing this family (179)
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| CN1925855B (zh) | 2003-12-19 | 2010-06-16 | 普莱希科公司 | 开发Ret调节剂的化合物和方法 |
| NZ584499A (en) | 2004-03-30 | 2011-08-26 | Vertex Pharma | Azaindoles Useful as Inhibitors of Jak and Other Protein Kinases |
| US7498342B2 (en) | 2004-06-17 | 2009-03-03 | Plexxikon, Inc. | Compounds modulating c-kit activity |
| US7361763B2 (en) | 2004-07-27 | 2008-04-22 | Sgx Pharmaceuticals, Inc. | Pyrrolo-pyridine kinase modulators |
| US7361764B2 (en) * | 2004-07-27 | 2008-04-22 | Sgx Pharmaceuticals, Inc. | Pyrrolo-pyridine kinase modulators |
| BRPI0513899A (pt) | 2004-07-27 | 2008-05-20 | Sgx Pharmaceuticals Inc | moduladores de cinase heterocìclica de anel fundido |
| US7626021B2 (en) | 2004-07-27 | 2009-12-01 | Sgx Pharmaceuticals, Inc. | Fused ring heterocycle kinase modulators |
| HN2005000795A (es) * | 2004-10-15 | 2010-08-19 | Aventis Pharma Inc | Pirimidinas como antagonistas del receptor de prostaglandina d2 |
| WO2006050076A1 (en) * | 2004-10-29 | 2006-05-11 | Janssen Pharmaceutica, N.V. | Pyrimidinyl substituted fused-pyrrolyl compounds useful in treating kinase disorders |
| US20090233955A1 (en) | 2004-12-08 | 2009-09-17 | Frazee James S | 1H-Pyrrolo[2,3-B]Pyridnes |
| CA2590250A1 (en) * | 2004-12-14 | 2006-06-22 | Vertex Pharmaceuticals Incorporated | Pyrimidine inhibitors of erk protein kinase and uses therof |
| SI1853588T1 (sl) | 2005-02-16 | 2008-10-31 | Astrazeneca Ab | Kemične spojine |
| US20060183758A1 (en) * | 2005-02-17 | 2006-08-17 | Cb Research And Development, Inc. | Method for synthesis of AZA-annelated pyrroles, thiophenes, and furans |
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| NZ564065A (en) | 2005-05-20 | 2011-03-31 | Vertex Pharma | Pyrrolopyridines useful as inhibitors of protein kinase |
| PL2395004T3 (pl) | 2005-06-22 | 2016-08-31 | Plexxikon Inc | Pochodne pirolo[2,3-b]pirydyny jako inhibitory kinazy białkowej |
| JP5119154B2 (ja) | 2005-09-22 | 2013-01-16 | インサイト・コーポレイション | Ｊａｎｕｓキナーゼの四環系阻害剤 |
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| TWI630207B (zh) | 2005-12-13 | 2018-07-21 | 英塞特控股公司 | 作為傑納斯激酶（ＪＡＮＵＳ ＫＩＮＡＳＥ）抑制劑之經雜芳基取代之吡咯并〔２，３-ｂ〕吡啶及吡咯并〔２，３-ｂ〕嘧啶 |
| MX2008008320A (es) * | 2005-12-23 | 2008-09-03 | Smithkline Beecham Corp | Inhibidores de azaindol de aurora cinasas. |
| AR060316A1 (es) * | 2006-01-17 | 2008-06-11 | Vertex Pharma | Azaindoles de utilidad como inhibidores de janus quinasas |
| US20070208053A1 (en) * | 2006-01-19 | 2007-09-06 | Arnold Lee D | Fused heterobicyclic kinase inhibitors |
| DE102006012617A1 (de) * | 2006-03-20 | 2007-09-27 | Merck Patent Gmbh | 4-(Pyrrolopyridinyl)-pyrimidinyl-2-amin-derivate |
| CN101460499A (zh) * | 2006-04-05 | 2009-06-17 | 沃泰克斯药物股份有限公司 | 可用作janus激酶抑制剂的去氮杂嘌呤 |
| US8604031B2 (en) * | 2006-05-18 | 2013-12-10 | Mannkind Corporation | Intracellular kinase inhibitors |
| CN101573335A (zh) * | 2006-10-09 | 2009-11-04 | 武田药品工业株式会社 | 激酶抑制剂 |
| EP2079696A2 (en) * | 2006-10-09 | 2009-07-22 | Takeda San Diego, Inc. | Kinase inhibitors |
| GEP20135728B (en) | 2006-10-09 | 2013-01-25 | Takeda Pharmaceuticals Co | Kinase inhibitors |
| WO2008063888A2 (en) | 2006-11-22 | 2008-05-29 | Plexxikon, Inc. | Compounds modulating c-fms and/or c-kit activity and uses therefor |
| PE20081581A1 (es) | 2006-12-21 | 2008-11-12 | Plexxikon Inc | COMPUESTOS PIRROLO[2,3-b]PIRIDINAS COMO MODULADORES DE QUINASA |
| WO2008079909A1 (en) * | 2006-12-21 | 2008-07-03 | Plexxikon, Inc. | Pyrrolo [2,3-b] pyridines as kinase modulators |
| US7872018B2 (en) | 2006-12-21 | 2011-01-18 | Plexxikon, Inc. | Compounds and methods for kinase modulation, and indications therefor |
| US8247421B2 (en) * | 2006-12-21 | 2012-08-21 | Vertex Pharmaceuticals Incorporated | 5-cyano-4-(pyrrolo [2,3B] pyridine-3-yl)-pyrimidine derivatives useful as protein kinase inhibitors |
| EP2121692B1 (en) | 2006-12-22 | 2013-04-10 | Incyte Corporation | Substituted heterocycles as janus kinase inhibitors |
| CN101778825A (zh) * | 2007-03-22 | 2010-07-14 | 沃泰克斯药物股份有限公司 | 适用作詹纳斯激酶抑制剂的n-杂环类化合物 |
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| CA2704199C (en) * | 2007-11-01 | 2016-01-19 | Acucela Inc. | Amine derivative compounds for treating ophthalmic diseases and disorders |
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| PL2288610T3 (pl) | 2008-03-11 | 2017-12-29 | Incyte Holdings Corporation | Azetydynowe i cyklobutanowe pochodne jako inhibitory jak |
| US8138339B2 (en) | 2008-04-16 | 2012-03-20 | Portola Pharmaceuticals, Inc. | Inhibitors of protein kinases |
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- 2005-03-30 CN CN201310486314.2A patent/CN103554104A/zh active Pending
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