JP2006514006A5 - - Google Patents
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- JP2006514006A5 JP2006514006A5 JP2004550483A JP2004550483A JP2006514006A5 JP 2006514006 A5 JP2006514006 A5 JP 2006514006A5 JP 2004550483 A JP2004550483 A JP 2004550483A JP 2004550483 A JP2004550483 A JP 2004550483A JP 2006514006 A5 JP2006514006 A5 JP 2006514006A5
- Authority
- JP
- Japan
- Prior art keywords
- substituted
- aliphatic
- phenyl
- drugs
- disease
- 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.)
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- 125000001931 aliphatic group Chemical group 0.000 claims description 27
- -1 t- butyl Chemical group 0.000 claims description 21
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims description 15
- 229910052739 hydrogen Inorganic materials 0.000 claims description 11
- 229910052757 nitrogen Inorganic materials 0.000 claims description 11
- IJGRMHOSHXDMSA-UHFFFAOYSA-N nitrogen Substances N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims description 11
- 239000001257 hydrogen Substances 0.000 claims description 10
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims description 10
- 125000001424 substituent group Chemical group 0.000 claims description 10
- 229910052760 oxygen Inorganic materials 0.000 claims description 8
- 229910052717 sulfur Chemical group 0.000 claims description 8
- NINIDFKCEFEMDL-UHFFFAOYSA-N Sulfur Chemical group [S] NINIDFKCEFEMDL-UHFFFAOYSA-N 0.000 claims description 7
- QVGXLLKOCUKJST-UHFFFAOYSA-N atomic oxygen Chemical group [O] QVGXLLKOCUKJST-UHFFFAOYSA-N 0.000 claims description 7
- 125000005842 heteroatom Chemical group 0.000 claims description 7
- 239000001301 oxygen Chemical group 0.000 claims description 7
- 239000011593 sulfur Chemical group 0.000 claims description 7
- 229910052736 halogen Inorganic materials 0.000 claims description 6
- 150000002367 halogens Chemical class 0.000 claims description 6
- 229920006395 saturated elastomer Polymers 0.000 claims description 6
- 125000006570 (C5-C6) heteroaryl group Chemical group 0.000 claims description 4
- 125000003118 aryl group Chemical group 0.000 claims description 4
- 125000001072 heteroaryl group Chemical group 0.000 claims description 4
- 125000000623 heterocyclic group Chemical group 0.000 claims description 4
- 125000004429 atom Chemical group 0.000 claims description 3
- 125000002619 bicyclic group Chemical group 0.000 claims description 3
- 125000002950 monocyclic group Chemical group 0.000 claims description 3
- 239000003814 drug Substances 0.000 claims 23
- 229940124597 therapeutic agent Drugs 0.000 claims 12
- 150000001875 compounds Chemical class 0.000 claims 11
- 229940079593 drug Drugs 0.000 claims 10
- 125000000217 alkyl group Chemical group 0.000 claims 6
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 6
- 239000000203 mixture Substances 0.000 claims 6
- 201000006417 multiple sclerosis Diseases 0.000 claims 6
- QJGQUHMNIGDVPM-UHFFFAOYSA-N nitrogen group Chemical group [N] QJGQUHMNIGDVPM-UHFFFAOYSA-N 0.000 claims 5
- 208000006673 asthma Diseases 0.000 claims 4
- 208000019995 familial amyotrophic lateral sclerosis Diseases 0.000 claims 4
- 125000005843 halogen group Chemical group 0.000 claims 4
- 201000010099 disease Diseases 0.000 claims 3
- 208000035475 disorder Diseases 0.000 claims 3
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 3
- 208000024827 Alzheimer disease Diseases 0.000 claims 2
- 208000023275 Autoimmune disease Diseases 0.000 claims 2
- 208000019838 Blood disease Diseases 0.000 claims 2
- 208000020084 Bone disease Diseases 0.000 claims 2
- 208000009329 Graft vs Host Disease Diseases 0.000 claims 2
- 208000002250 Hematologic Neoplasms Diseases 0.000 claims 2
- 206010020751 Hypersensitivity Diseases 0.000 claims 2
- 208000029462 Immunodeficiency disease Diseases 0.000 claims 2
- 206010025323 Lymphomas Diseases 0.000 claims 2
- 108010025020 Nerve Growth Factor Proteins 0.000 claims 2
- 102000007072 Nerve Growth Factors Human genes 0.000 claims 2
- 208000018737 Parkinson disease Diseases 0.000 claims 2
- 206010052779 Transplant rejections Diseases 0.000 claims 2
- 102100025387 Tyrosine-protein kinase JAK3 Human genes 0.000 claims 2
- 230000000172 allergic effect Effects 0.000 claims 2
- 229940124599 anti-inflammatory drug Drugs 0.000 claims 2
- 230000001028 anti-proliverative effect Effects 0.000 claims 2
- 125000006615 aromatic heterocyclic group Chemical group 0.000 claims 2
- 150000001721 carbon Chemical class 0.000 claims 2
- 230000001066 destructive effect Effects 0.000 claims 2
- 230000000694 effects Effects 0.000 claims 2
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims 2
- 208000024908 graft versus host disease Diseases 0.000 claims 2
- 208000014951 hematologic disease Diseases 0.000 claims 2
- 208000018706 hematopoietic system disease Diseases 0.000 claims 2
- 230000028993 immune response Effects 0.000 claims 2
- 239000002955 immunomodulating agent Substances 0.000 claims 2
- 229940121354 immunomodulator Drugs 0.000 claims 2
- 229960003444 immunosuppressant agent Drugs 0.000 claims 2
- 239000003018 immunosuppressive agent Substances 0.000 claims 2
- 230000002401 inhibitory effect Effects 0.000 claims 2
- 208000032839 leukemia Diseases 0.000 claims 2
- 208000019423 liver disease Diseases 0.000 claims 2
- 238000000034 method Methods 0.000 claims 2
- 230000004770 neurodegeneration Effects 0.000 claims 2
- 239000003900 neurotrophic factor Substances 0.000 claims 2
- 125000004433 nitrogen atom Chemical group N* 0.000 claims 2
- 125000000951 phenoxy group Chemical group [H]C1=C([H])C([H])=C(O*)C([H])=C1[H] 0.000 claims 2
- 125000004076 pyridyl group Chemical group 0.000 claims 2
- 206010039073 rheumatoid arthritis Diseases 0.000 claims 2
- 201000000980 schizophrenia Diseases 0.000 claims 2
- 239000007787 solid Substances 0.000 claims 2
- 101000934996 Homo sapiens Tyrosine-protein kinase JAK3 Proteins 0.000 claims 1
- 206010028289 Muscle atrophy Diseases 0.000 claims 1
- ISWSIDIOOBJBQZ-UHFFFAOYSA-N Phenol Chemical compound OC1=CC=CC=C1 ISWSIDIOOBJBQZ-UHFFFAOYSA-N 0.000 claims 1
- 101710112792 Tyrosine-protein kinase JAK3 Proteins 0.000 claims 1
- 239000002671 adjuvant Substances 0.000 claims 1
- 125000001118 alkylidene group Chemical group 0.000 claims 1
- 208000030961 allergic reaction Diseases 0.000 claims 1
- 206010002026 amyotrophic lateral sclerosis Diseases 0.000 claims 1
- 239000002246 antineoplastic agent Substances 0.000 claims 1
- 208000010216 atopic IgE responsiveness Diseases 0.000 claims 1
- 208000010668 atopic eczema Diseases 0.000 claims 1
- 125000001797 benzyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])* 0.000 claims 1
- 125000000051 benzyloxy group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])O* 0.000 claims 1
- 239000012472 biological sample Substances 0.000 claims 1
- 229910052794 bromium Inorganic materials 0.000 claims 1
- 229910052799 carbon Inorganic materials 0.000 claims 1
- 125000006297 carbonyl amino group Chemical group [H]N([*:2])C([*:1])=O 0.000 claims 1
- 239000002327 cardiovascular agent Substances 0.000 claims 1
- 229940125692 cardiovascular agent Drugs 0.000 claims 1
- 239000003795 chemical substances by application Substances 0.000 claims 1
- 230000000973 chemotherapeutic effect Effects 0.000 claims 1
- 229910052801 chlorine Inorganic materials 0.000 claims 1
- 125000000068 chlorophenyl group Chemical group 0.000 claims 1
- 125000000113 cyclohexyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])(*)C([H])([H])C1([H])[H] 0.000 claims 1
- 125000001511 cyclopentyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])(*)C1([H])[H] 0.000 claims 1
- 125000001559 cyclopropyl group Chemical group [H]C1([H])C([H])([H])C1([H])* 0.000 claims 1
- 229940127089 cytotoxic agent Drugs 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 230000002526 effect on cardiovascular system Effects 0.000 claims 1
- 229910052731 fluorine Inorganic materials 0.000 claims 1
- 125000001207 fluorophenyl group Chemical group 0.000 claims 1
- 201000005787 hematologic cancer Diseases 0.000 claims 1
- 208000024200 hematopoietic and lymphoid system neoplasm Diseases 0.000 claims 1
- 125000004051 hexyl group Chemical group [H]C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])* 0.000 claims 1
- 125000001449 isopropyl group Chemical group [H]C([H])([H])C([H])(*)C([H])([H])[H] 0.000 claims 1
- 201000010901 lateral sclerosis Diseases 0.000 claims 1
- 238000004519 manufacturing process Methods 0.000 claims 1
- 125000000325 methylidene group Chemical group [H]C([H])=* 0.000 claims 1
- 208000005264 motor neuron disease Diseases 0.000 claims 1
- 230000020763 muscle atrophy Effects 0.000 claims 1
- 201000000585 muscular atrophy Diseases 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
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 claims 1
- 125000001147 pentyl group Chemical group C(CCCC)* 0.000 claims 1
- 239000008194 pharmaceutical composition Substances 0.000 claims 1
- 125000004193 piperazinyl group Chemical group 0.000 claims 1
- 125000001436 propyl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])[H] 0.000 claims 1
- 150000003839 salts Chemical class 0.000 claims 1
- 239000000523 sample Substances 0.000 claims 1
- 125000000999 tert-butyl group Chemical group [H]C([H])([H])C(*)(C([H])([H])[H])C([H])([H])[H] 0.000 claims 1
- 229940126585 therapeutic drug Drugs 0.000 claims 1
- 239000003981 vehicle Substances 0.000 claims 1
- 125000003710 aryl alkyl group Chemical group 0.000 description 1
- 125000005160 aryl oxy alkyl group Chemical group 0.000 description 1
- 125000004432 carbon atom Chemical group C* 0.000 description 1
- 125000004475 heteroaralkyl group Chemical group 0.000 description 1
- 125000005114 heteroarylalkoxy group Chemical group 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US42357902P | 2002-11-04 | 2002-11-04 | |
| US60/423,579 | 2002-11-04 | ||
| PCT/US2003/035163 WO2004041814A1 (en) | 2002-11-04 | 2003-11-04 | Heteroaryl-pyramidine derivatives as jak inhibitors |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2010211038A Division JP2011016839A (ja) | 2002-11-04 | 2010-09-21 | Ｊａｋインヒビターとしてのヘテロアリール−ピリミジン誘導体 |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2006514006A JP2006514006A (ja) | 2006-04-27 |
| JP2006514006A5 true JP2006514006A5 (enExample) | 2010-06-03 |
| JP4688498B2 JP4688498B2 (ja) | 2011-05-25 |
Family
ID=32312681
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2004550483A Expired - Fee Related JP4688498B2 (ja) | 2002-11-04 | 2003-11-04 | Ｊａｋインヒビターとしてのヘテロアリール−ピリミジン誘導体 |
| JP2010211038A Pending JP2011016839A (ja) | 2002-11-04 | 2010-09-21 | Ｊａｋインヒビターとしてのヘテロアリール−ピリミジン誘導体 |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2010211038A Pending JP2011016839A (ja) | 2002-11-04 | 2010-09-21 | Ｊａｋインヒビターとしてのヘテロアリール−ピリミジン誘導体 |
Country Status (9)
| Country | Link |
|---|---|
| US (1) | US7259161B2 (enExample) |
| EP (1) | EP1562938B1 (enExample) |
| JP (2) | JP4688498B2 (enExample) |
| AT (1) | ATE371656T1 (enExample) |
| AU (1) | AU2003295396B2 (enExample) |
| CA (1) | CA2506773A1 (enExample) |
| DE (1) | DE60316013T2 (enExample) |
| ES (1) | ES2289349T3 (enExample) |
| WO (1) | WO2004041814A1 (enExample) |
Families Citing this family (87)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| AU2001290912A1 (en) * | 2000-09-15 | 2002-03-26 | Vertex Pharmaceuticals Incorporated | Pyrazole compounds useful as protein kinase inhibitors |
| TWI329105B (en) | 2002-02-01 | 2010-08-21 | Rigel Pharmaceuticals Inc | 2,4-pyrimidinediamine compounds and their uses |
| IL166241A0 (en) * | 2002-07-29 | 2006-01-15 | Rigel Pharmaceuticals Inc | Method of treating or preventing autoimmune diseases with 2,4-pyrimidinedinediamine compounds |
| ES2421139T3 (es) | 2003-07-30 | 2013-08-29 | Rigel Pharmaceuticals, Inc. | Compuestos de 2,4-pirimidindiamina para su uso en el tratamiento o la prevención de enfermedades autoinmunitarias |
| RU2007107177A (ru) * | 2004-07-28 | 2008-09-10 | Айрм Ллк (Bm) | Соединения и композиции, как модуляторы ядерных рецепторов стероидных гормонов |
| CA2584167A1 (en) | 2004-10-22 | 2006-05-04 | Amgen Inc. | Substituted nitrogen-containing heterocycles as vanilloid receptor ligands and their uses as medicament |
| ATE540035T1 (de) | 2004-11-24 | 2012-01-15 | Rigel Pharmaceuticals Inc | Spiro-2,4-pyrimidindiamin-verbindungen und ihre verwendungen |
| KR101389300B1 (ko) | 2005-02-14 | 2014-04-25 | 존슨 앤드 존슨 비젼 케어, 인코포레이티드 | 안과용 렌즈의 제조방법, 안과용 장치 및 콘택트 렌즈 |
| JP2008540436A (ja) * | 2005-05-03 | 2008-11-20 | ライジェル ファーマシューティカルズ， インコーポレイテッド | Ｊａｋキナーゼインヒビターおよびそれらの使用 |
| WO2006133426A2 (en) | 2005-06-08 | 2006-12-14 | Rigel Pharmaceuticals, Inc. | Compositions and methods for inhibition of the jak pathway |
| US20070203161A1 (en) | 2006-02-24 | 2007-08-30 | Rigel Pharmaceuticals, Inc. | Compositions and methods for inhibition of the jak pathway |
| WO2007053452A1 (en) | 2005-11-01 | 2007-05-10 | Targegen, Inc. | Bi-aryl meta-pyrimidine inhibitors of kinases |
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| US8969295B2 (en) * | 2006-04-14 | 2015-03-03 | Massachusetts Institute Of Technology | Identifying and modulating molecular pathways that mediate nervous system plasticity |
| DK2089369T3 (da) | 2006-10-19 | 2011-05-09 | Rigel Pharmaceuticals Inc | 2,4-pyrimidindiaminderivater som hæmmere af JAK-kinaser til behandling af autoimmune sygdomme |
| ES2415863T3 (es) | 2006-12-22 | 2013-07-29 | Incyte Corporation | Heterociclos sustituidos como inhibidores de Janus Quinasas |
| HUE029188T2 (en) | 2007-03-12 | 2017-03-28 | Ym Biosciences Australia Pty | Phenylamino-pyrimidine compounds and their use |
| JP5676249B2 (ja) | 2007-04-20 | 2015-02-25 | プロビオドルグ エージー | グルタミニルシクラーゼ阻害剤としてのアミノピリジン誘導体 |
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| US20090048282A1 (en) * | 2007-08-14 | 2009-02-19 | Wyeth | Pyrimidine sulfonamide analogs and their use as agonists of the wnt-beta-catenin cellular messaging system |
| EP2200436B1 (en) * | 2007-09-04 | 2015-01-21 | The Scripps Research Institute | Substituted pyrimidinyl-amines as protein kinase inhibitors |
| HRP20170317T1 (hr) | 2008-02-15 | 2017-04-21 | Rigel Pharmaceuticals, Inc. | Spojevi pirimidin-2-amina i njihova uporaba kao inhibitora jak kinaza |
| MY165582A (en) | 2008-03-11 | 2018-04-05 | Incyte Holdings Corp | Azetidine and cyclobutane derivatives as jak inhibitors |
| US8138339B2 (en) | 2008-04-16 | 2012-03-20 | Portola Pharmaceuticals, Inc. | Inhibitors of protein kinases |
| US8063058B2 (en) | 2008-04-16 | 2011-11-22 | Portola Pharmaceuticals, Inc. | Inhibitors of syk and JAK protein kinases |
| BRPI0910668A2 (pt) | 2008-04-22 | 2019-09-24 | Portola Pharmaceutiacals Inc | inibidores de proteína quinases |
| 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 |
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| AR081626A1 (es) | 2010-04-23 | 2012-10-10 | Cytokinetics Inc | Compuestos amino-piridazinicos, composiciones farmaceuticas que los contienen y uso de los mismos para tratar trastornos musculares cardiacos y esqueleticos |
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| AR081331A1 (es) | 2010-04-23 | 2012-08-08 | Cytokinetics Inc | Amino- pirimidinas composiciones de las mismas y metodos para el uso de los mismos |
| EA202091303A3 (ru) | 2010-05-21 | 2021-05-31 | Инсайт Холдингс Корпорейшн | Композиция ингибитора jak для местного применения |
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| US8691807B2 (en) | 2011-06-20 | 2014-04-08 | Incyte Corporation | Azetidinyl phenyl, pyridyl or pyrazinyl carboxamide derivatives as JAK inhibitors |
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| US8809359B2 (en) | 2012-06-29 | 2014-08-19 | Ym Biosciences Australia Pty Ltd | Phenyl amino pyrimidine bicyclic compounds and uses thereof |
| WO2014013014A1 (en) | 2012-07-18 | 2014-01-23 | Fundació Privada Centre De Regulació Genòmica (Crg) | Jak inhibitors for activation of epidermal stem cell populations |
| WO2014058921A2 (en) | 2012-10-08 | 2014-04-17 | Portola Pharmaceuticals, Inc. | Substituted pyrimidinyl kinase inhibitors |
| KR102242077B1 (ko) | 2012-11-15 | 2021-04-20 | 인사이트 홀딩스 코포레이션 | 룩솔리티니브의 서방성 제형 |
| EP3489239B1 (en) | 2013-03-06 | 2021-09-15 | Incyte Holdings Corporation | Processes and intermediates for making a jak inhibitor |
| RS62649B1 (sr) | 2013-03-12 | 2021-12-31 | Vertex Pharma | Inhibitori dnk-pk |
| 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). |
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2003
- 2003-11-04 US US10/700,936 patent/US7259161B2/en not_active Expired - Fee Related
- 2003-11-04 DE DE60316013T patent/DE60316013T2/de not_active Expired - Lifetime
- 2003-11-04 EP EP03786582A patent/EP1562938B1/en not_active Expired - Lifetime
- 2003-11-04 ES ES03786582T patent/ES2289349T3/es not_active Expired - Lifetime
- 2003-11-04 JP JP2004550483A patent/JP4688498B2/ja not_active Expired - Fee Related
- 2003-11-04 WO PCT/US2003/035163 patent/WO2004041814A1/en not_active Ceased
- 2003-11-04 AT AT03786582T patent/ATE371656T1/de not_active IP Right Cessation
- 2003-11-04 AU AU2003295396A patent/AU2003295396B2/en not_active Ceased
- 2003-11-04 CA CA002506773A patent/CA2506773A1/en not_active Abandoned
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2010
- 2010-09-21 JP JP2010211038A patent/JP2011016839A/ja active Pending