JP2006514989A5 - - Google Patents
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- JP2006514989A5 JP2006514989A5 JP2005506142A JP2005506142A JP2006514989A5 JP 2006514989 A5 JP2006514989 A5 JP 2006514989A5 JP 2005506142 A JP2005506142 A JP 2005506142A JP 2005506142 A JP2005506142 A JP 2005506142A JP 2006514989 A5 JP2006514989 A5 JP 2006514989A5
- Authority
- JP
- Japan
- Prior art keywords
- group
- use according
- phenyl
- autoimmune
- 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.)
- Pending
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- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims description 18
- 150000001875 compounds Chemical class 0.000 claims description 8
- 125000003545 alkoxy group Chemical group 0.000 claims description 3
- 229910052736 halogen Inorganic materials 0.000 claims description 3
- 150000002367 halogens Chemical class 0.000 claims description 3
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims description 2
- -1 monosubstituted phenyl Chemical group 0.000 claims 15
- 208000023275 Autoimmune disease Diseases 0.000 claims 11
- 229910052739 hydrogen Inorganic materials 0.000 claims 9
- 239000001257 hydrogen Substances 0.000 claims 9
- 125000000217 alkyl group Chemical group 0.000 claims 8
- 125000001072 heteroaryl group Chemical group 0.000 claims 8
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 6
- 230000001363 autoimmune Effects 0.000 claims 6
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 claims 5
- 229910052760 oxygen Inorganic materials 0.000 claims 5
- KAESVJOAVNADME-UHFFFAOYSA-N 1H-pyrrole Natural products C=1C=CNC=1 KAESVJOAVNADME-UHFFFAOYSA-N 0.000 claims 4
- 125000003710 aryl alkyl group Chemical group 0.000 claims 4
- SIKJAQJRHWYJAI-UHFFFAOYSA-N benzopyrrole Natural products C1=CC=C2NC=CC2=C1 SIKJAQJRHWYJAI-UHFFFAOYSA-N 0.000 claims 4
- 239000003814 drug Substances 0.000 claims 4
- 150000004677 hydrates Chemical class 0.000 claims 4
- 150000003839 salts Chemical class 0.000 claims 4
- 230000009885 systemic effect Effects 0.000 claims 4
- 125000000008 (C1-C10) alkyl group Chemical group 0.000 claims 3
- 125000001313 C5-C10 heteroaryl group Chemical group 0.000 claims 3
- 150000001204 N-oxides Chemical class 0.000 claims 3
- 125000003118 aryl group Chemical group 0.000 claims 3
- 229910052799 carbon Inorganic materials 0.000 claims 3
- 125000004432 carbon atom Chemical group C* 0.000 claims 3
- 125000004093 cyano group Chemical group *C#N 0.000 claims 3
- PZOUSPYUWWUPPK-UHFFFAOYSA-N indole Natural products CC1=CC=CC2=C1C=CN2 PZOUSPYUWWUPPK-UHFFFAOYSA-N 0.000 claims 3
- RKJUIXBNRJVNHR-UHFFFAOYSA-N indolenine Natural products C1=CC=C2CC=NC2=C1 RKJUIXBNRJVNHR-UHFFFAOYSA-N 0.000 claims 3
- 229910052757 nitrogen Inorganic materials 0.000 claims 3
- 239000012453 solvate Substances 0.000 claims 3
- 229910052717 sulfur Inorganic materials 0.000 claims 3
- 125000006552 (C3-C8) cycloalkyl group Chemical group 0.000 claims 2
- IANQTJSKSUMEQM-UHFFFAOYSA-N 1-benzofuran Chemical compound C1=CC=C2OC=CC2=C1 IANQTJSKSUMEQM-UHFFFAOYSA-N 0.000 claims 2
- 208000004300 Atrophic Gastritis Diseases 0.000 claims 2
- 206010050245 Autoimmune thrombocytopenia Diseases 0.000 claims 2
- 208000023328 Basedow disease Diseases 0.000 claims 2
- 208000008439 Biliary Liver Cirrhosis Diseases 0.000 claims 2
- 208000033222 Biliary cirrhosis primary Diseases 0.000 claims 2
- 125000000172 C5-C10 aryl group Chemical group 0.000 claims 2
- 206010008909 Chronic Hepatitis Diseases 0.000 claims 2
- 208000036495 Gastritis atrophic Diseases 0.000 claims 2
- 208000024869 Goodpasture syndrome Diseases 0.000 claims 2
- 208000015023 Graves' disease Diseases 0.000 claims 2
- 208000030836 Hashimoto thyroiditis Diseases 0.000 claims 2
- 208000035186 Hemolytic Autoimmune Anemia Diseases 0.000 claims 2
- 206010019755 Hepatitis chronic active Diseases 0.000 claims 2
- 208000031845 Pernicious anaemia Diseases 0.000 claims 2
- 208000012654 Primary biliary cholangitis Diseases 0.000 claims 2
- 206010042742 Sympathetic ophthalmia Diseases 0.000 claims 2
- 208000031981 Thrombocytopenic Idiopathic Purpura Diseases 0.000 claims 2
- 201000000448 autoimmune hemolytic anemia Diseases 0.000 claims 2
- 125000001797 benzyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])* 0.000 claims 2
- 208000016644 chronic atrophic gastritis Diseases 0.000 claims 2
- 125000001316 cycloalkyl alkyl group Chemical group 0.000 claims 2
- 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 2
- 239000003085 diluting agent Substances 0.000 claims 2
- 201000002491 encephalomyelitis Diseases 0.000 claims 2
- 125000004438 haloalkoxy group Chemical group 0.000 claims 2
- 125000004404 heteroalkyl group Chemical group 0.000 claims 2
- 125000004446 heteroarylalkyl group Chemical group 0.000 claims 2
- 150000002431 hydrogen Chemical class 0.000 claims 2
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 2
- 150000002475 indoles Chemical class 0.000 claims 2
- 206010025135 lupus erythematosus Diseases 0.000 claims 2
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 2
- 125000002757 morpholinyl group Chemical group 0.000 claims 2
- 201000006417 multiple sclerosis Diseases 0.000 claims 2
- 206010028417 myasthenia gravis Diseases 0.000 claims 2
- 201000005737 orchitis Diseases 0.000 claims 2
- 239000000546 pharmaceutical excipient Substances 0.000 claims 2
- 125000004193 piperazinyl group Chemical group 0.000 claims 2
- 125000003386 piperidinyl group Chemical group 0.000 claims 2
- 150000003233 pyrroles Chemical class 0.000 claims 2
- 206010039073 rheumatoid arthritis Diseases 0.000 claims 2
- 125000001424 substituent group Chemical group 0.000 claims 2
- 125000006677 (C1-C3) haloalkoxy group Chemical group 0.000 claims 1
- 125000006583 (C1-C3) haloalkyl group Chemical group 0.000 claims 1
- 125000006664 (C1-C3) perfluoroalkyl group Chemical group 0.000 claims 1
- 125000004191 (C1-C6) alkoxy group Chemical group 0.000 claims 1
- 125000006708 (C5-C14) heteroaryl group Chemical group 0.000 claims 1
- RYHBNJHYFVUHQT-UHFFFAOYSA-N 1,4-Dioxane Chemical compound C1COCCO1 RYHBNJHYFVUHQT-UHFFFAOYSA-N 0.000 claims 1
- LJRUKUQEIHJTEL-UHFFFAOYSA-N 2,2-dimethyl-4h-1,4-benzoxazin-3-one Chemical compound C1=CC=C2NC(=O)C(C)(C)OC2=C1 LJRUKUQEIHJTEL-UHFFFAOYSA-N 0.000 claims 1
- AJKPUNIYEMWTIL-UHFFFAOYSA-N 2-[5-[[4-[(2,2-difluoro-3-oxo-4H-1,4-benzoxazin-6-yl)amino]-5-fluoropyrimidin-2-yl]amino]-2-methylcyclohexa-1,5-dien-1-yl]oxy-N-methylacetamide Chemical compound CNC(=O)COC1=C(C)CCC(Nc2ncc(F)c(Nc3ccc4OC(F)(F)C(=O)Nc4c3)n2)=C1 AJKPUNIYEMWTIL-UHFFFAOYSA-N 0.000 claims 1
- VDYYZYAHNFWOPX-UHFFFAOYSA-N 2-n,4-n-bis(3-aminophenyl)-5-fluoropyrimidine-2,4-diamine Chemical compound NC1=CC=CC(NC=2N=C(NC=3C=C(N)C=CC=3)C(F)=CN=2)=C1 VDYYZYAHNFWOPX-UHFFFAOYSA-N 0.000 claims 1
- PVTXJGJDOHYFOX-UHFFFAOYSA-N 2h-1,4-benzoxazine Chemical compound C1=CC=C2N=CCOC2=C1 PVTXJGJDOHYFOX-UHFFFAOYSA-N 0.000 claims 1
- YHWMFDLNZGIJSD-UHFFFAOYSA-N 2h-1,4-oxazine Chemical compound C1OC=CN=C1 YHWMFDLNZGIJSD-UHFFFAOYSA-N 0.000 claims 1
- VMUXSMXIQBNMGZ-UHFFFAOYSA-N 3,4-dihydrocoumarin Chemical compound C1=CC=C2OC(=O)CCC2=C1 VMUXSMXIQBNMGZ-UHFFFAOYSA-N 0.000 claims 1
- XISPDFMAOWZEQG-UHFFFAOYSA-N 4h-1,4-oxazin-3-one Chemical compound O=C1COC=CN1 XISPDFMAOWZEQG-UHFFFAOYSA-N 0.000 claims 1
- KYNSBQPICQTCGU-UHFFFAOYSA-N Benzopyrane Chemical compound C1=CC=C2C=CCOC2=C1 KYNSBQPICQTCGU-UHFFFAOYSA-N 0.000 claims 1
- 241000248040 Globulosis Species 0.000 claims 1
- 206010034277 Pemphigoid Diseases 0.000 claims 1
- 229920001774 Perfluoroether Polymers 0.000 claims 1
- 206010036790 Productive cough Diseases 0.000 claims 1
- 208000033464 Reiter syndrome Diseases 0.000 claims 1
- 208000021386 Sjogren Syndrome Diseases 0.000 claims 1
- 201000009594 Systemic Scleroderma Diseases 0.000 claims 1
- 206010042953 Systemic sclerosis Diseases 0.000 claims 1
- 125000002877 alkyl aryl group Chemical group 0.000 claims 1
- 125000004103 aminoalkyl group Chemical group 0.000 claims 1
- 125000005605 benzo group Chemical group 0.000 claims 1
- QRUDEWIWKLJBPS-UHFFFAOYSA-N benzotriazole Chemical compound C1=CC=C2N[N][N]C2=C1 QRUDEWIWKLJBPS-UHFFFAOYSA-N 0.000 claims 1
- 125000004622 benzoxazinyl group Chemical group O1NC(=CC2=C1C=CC=C2)* 0.000 claims 1
- 208000000594 bullous pemphigoid Diseases 0.000 claims 1
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 claims 1
- 238000006243 chemical reaction Methods 0.000 claims 1
- ZYGHJZDHTFUPRJ-UHFFFAOYSA-N coumarin Chemical compound C1=CC=C2OC(=O)C=CC2=C1 ZYGHJZDHTFUPRJ-UHFFFAOYSA-N 0.000 claims 1
- 125000004122 cyclic group Chemical group 0.000 claims 1
- 201000001981 dermatomyositis Diseases 0.000 claims 1
- DMSHWWDRAYHEBS-UHFFFAOYSA-N dihydrocoumarin Natural products C1CC(=O)OC2=C1C=C(OC)C(OC)=C2 DMSHWWDRAYHEBS-UHFFFAOYSA-N 0.000 claims 1
- 229940079593 drug Drugs 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 150000002148 esters Chemical class 0.000 claims 1
- 125000001153 fluoro group Chemical group F* 0.000 claims 1
- 125000004428 fluoroalkoxy group Chemical group 0.000 claims 1
- 125000003709 fluoroalkyl group Chemical group 0.000 claims 1
- 125000005843 halogen group Chemical group 0.000 claims 1
- 125000005842 heteroatom Chemical group 0.000 claims 1
- 125000002768 hydroxyalkyl group Chemical group 0.000 claims 1
- LPAGFVYQRIESJQ-UHFFFAOYSA-N indoline Chemical compound C1=CC=C2NCCC2=C1 LPAGFVYQRIESJQ-UHFFFAOYSA-N 0.000 claims 1
- 201000008350 membranous glomerulonephritis Diseases 0.000 claims 1
- 125000000250 methylamino group Chemical group [H]N(*)C([H])([H])[H] 0.000 claims 1
- 239000000203 mixture Substances 0.000 claims 1
- 125000001624 naphthyl group Chemical group 0.000 claims 1
- 125000004433 nitrogen atom Chemical group N* 0.000 claims 1
- 125000004043 oxo group Chemical group O=* 0.000 claims 1
- 239000008194 pharmaceutical composition Substances 0.000 claims 1
- 201000006292 polyarteritis nodosa Diseases 0.000 claims 1
- YAAWASYJIRZXSZ-UHFFFAOYSA-N pyrimidine-2,4-diamine Chemical class NC1=CC=NC(N)=N1 YAAWASYJIRZXSZ-UHFFFAOYSA-N 0.000 claims 1
- 208000002574 reactive arthritis Diseases 0.000 claims 1
- 210000003802 sputum Anatomy 0.000 claims 1
- 208000024794 sputum Diseases 0.000 claims 1
- 238000002560 therapeutic procedure Methods 0.000 claims 1
- 0 C*(C=C1)C=CC(OC2(*)*)=C1NC2=O Chemical compound C*(C=C1)C=CC(OC2(*)*)=C1NC2=O 0.000 description 2
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US39967302P | 2002-07-29 | 2002-07-29 | |
| US44394903P | 2003-01-31 | 2003-01-31 | |
| US45233903P | 2003-03-06 | 2003-03-06 | |
| US10/631,029 US7517886B2 (en) | 2002-07-29 | 2003-07-29 | Methods of treating or preventing autoimmune diseases with 2,4-pyrimidinediamine compounds |
| PCT/US2003/024087 WO2004014382A1 (en) | 2002-07-29 | 2003-07-29 | Methods of treating or preventing autoimmune diseases with 2,4-pyrimidinediamine compounds |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2010152958A Division JP5441841B2 (ja) | 2002-07-29 | 2010-07-05 | 2,4−ピリミジンジアミン化合物による自己免疫疾患の処置または予防の方法 |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2006514989A JP2006514989A (ja) | 2006-05-18 |
| JP2006514989A5 true JP2006514989A5 (enExample) | 2010-08-19 |
Family
ID=31721742
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2005506142A Pending JP2006514989A (ja) | 2002-07-29 | 2003-07-29 | 2,4−ピリミジンジアミン化合物による自己免疫疾患の治療および予防方法 |
| JP2010152958A Expired - Fee Related JP5441841B2 (ja) | 2002-07-29 | 2010-07-05 | 2,4−ピリミジンジアミン化合物による自己免疫疾患の処置または予防の方法 |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2010152958A Expired - Fee Related JP5441841B2 (ja) | 2002-07-29 | 2010-07-05 | 2,4−ピリミジンジアミン化合物による自己免疫疾患の処置または予防の方法 |
Country Status (24)
| Country | Link |
|---|---|
| US (5) | US7517886B2 (enExample) |
| EP (1) | EP1534286B1 (enExample) |
| JP (2) | JP2006514989A (enExample) |
| CN (2) | CN103169708B (enExample) |
| AT (1) | ATE451104T1 (enExample) |
| AU (1) | AU2003265336B8 (enExample) |
| BR (1) | BR0313059B8 (enExample) |
| CA (1) | CA2492325C (enExample) |
| CY (1) | CY1110292T1 (enExample) |
| DE (1) | DE60330466D1 (enExample) |
| DK (1) | DK1534286T3 (enExample) |
| ES (2) | ES2445208T3 (enExample) |
| HR (1) | HRP20050089B1 (enExample) |
| IL (3) | IL166241A0 (enExample) |
| IS (1) | IS2923B (enExample) |
| MX (1) | MXPA05001096A (enExample) |
| NO (1) | NO332550B1 (enExample) |
| NZ (1) | NZ537752A (enExample) |
| PL (1) | PL216744B1 (enExample) |
| RS (1) | RS51752B (enExample) |
| RU (1) | RU2659777C9 (enExample) |
| SE (1) | SE0500203L (enExample) |
| SG (1) | SG176311A1 (enExample) |
| WO (1) | WO2004014382A1 (enExample) |
Families Citing this family (183)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| TWI329105B (en) * | 2002-02-01 | 2010-08-21 | Rigel Pharmaceuticals Inc | 2,4-pyrimidinediamine compounds and their uses |
| CN103169708B (zh) | 2002-07-29 | 2018-02-02 | 里格尔药品股份有限公司 | 用2,4‑嘧啶二胺化合物治疗或者预防自体免疫性疾病的方法 |
| WO2004048343A1 (en) * | 2002-11-28 | 2004-06-10 | Schering Aktiengesellschaft | Chk-, pdk- and akt-inhibitory pyrimidines, their production and use as pharmaceutical agents |
| UA80767C2 (en) * | 2002-12-20 | 2007-10-25 | Pfizer Prod Inc | Pyrimidine derivatives for the treatment of abnormal cell growth |
| CL2004000303A1 (es) * | 2003-02-20 | 2005-04-08 | Tibotec Pharm Ltd | Compuestos derivados de pirimidinas y triazinas; proceso de preparacion; composicion farmaceutica; y su uso para inhibir la replicacion del vih. |
| WO2005012262A1 (en) * | 2003-07-30 | 2005-02-10 | Cyclacel Limited | 2-aminophenyl-4-phenylpyrimidines as kinase inhibitors |
| US7122542B2 (en) | 2003-07-30 | 2006-10-17 | Rigel Pharmaceuticals, Inc. | Methods of treating or preventing autoimmune diseases with 2,4-pyrimidinediamine compounds |
| DK1663242T3 (da) * | 2003-08-07 | 2011-08-01 | Rigel Pharmaceuticals Inc | 2,4-Pyrimidindiamin-forbindelser og anvendelse som antiproliferative midler |
| JP4607879B2 (ja) * | 2003-08-15 | 2011-01-05 | ノバルティス アーゲー | 新生物疾患、炎症および免疫障害の処置に有用な2,4−ピリミジンジアミン |
| NZ551027A (en) | 2004-04-08 | 2011-01-28 | Targegen Inc | Benzotriazine inhibitors of kinases |
| JP4812763B2 (ja) | 2004-05-18 | 2011-11-09 | 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 | シクロアルキル置換ピリミジンジアミン化合物およびそれらの用途 |
| JP5275628B2 (ja) | 2004-08-25 | 2013-08-28 | ターゲジェン インコーポレーティッド | 複素環式化合物および使用方法 |
| US20060058525A1 (en) * | 2004-09-01 | 2006-03-16 | Rajinder Singh | Synthesis of 2,4-pyrimidinediamine compounds |
| CA2581454A1 (en) | 2004-09-23 | 2006-03-30 | Reddy Us Therapeutics, Inc. | Novel pyrimidine compounds, process for their preparation and compositions containing them |
| GB2420559B (en) | 2004-11-15 | 2008-08-06 | Rigel Pharmaceuticals Inc | Stereoisomerically enriched 3-aminocarbonyl bicycloheptene pyrimidinediamine compounds and their uses |
| ATE540035T1 (de) | 2004-11-24 | 2012-01-15 | Rigel Pharmaceuticals Inc | Spiro-2,4-pyrimidindiamin-verbindungen und ihre verwendungen |
| MY169441A (en) * | 2004-12-08 | 2019-04-11 | Janssen Pharmaceutica Nv | 2,4, (4,6) pyrimidine derivatives |
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| KR20070097590A (ko) | 2005-01-25 | 2007-10-04 | 에픽스 델라웨어, 인코포레이티드 | 치환된 아릴아민 화합물 및 5―ht6 조절제로서의 이의용도 |
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| US20070203161A1 (en) | 2006-02-24 | 2007-08-30 | Rigel Pharmaceuticals, Inc. | Compositions and methods for inhibition of the jak pathway |
| RU2485106C2 (ru) | 2005-06-08 | 2013-06-20 | Райджел Фамэсьютикэлз, Инк. | Соединения, проявляющие активность в отношении jak-киназы (варианты), способ лечения заболеваний, опосредованных jak-киназой, способ ингибирования активности jak-киназы (варианты), фармацевтическая композиция на основе указанных соединений |
| US7576053B2 (en) | 2005-06-13 | 2009-08-18 | Rigel Pharmaceuticals, Inc. | Methods and compositions for treating degenerative bone disorders |
| EP1890703B1 (en) * | 2005-06-14 | 2016-05-11 | Taigen Biotechnology | Pyrimidine compounds as chemokine receptors inhibitors |
| PT1734251E (pt) * | 2005-06-17 | 2007-03-30 | Magneti Marelli Powertrain Spa | Injector de combustível |
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| WO2007028445A1 (en) * | 2005-07-15 | 2007-03-15 | Glaxo Group Limited | 6-indolyl-4-yl-amino-5-halogeno-2-pyrimidinyl-amino derivatives |
| US8133900B2 (en) * | 2005-11-01 | 2012-03-13 | Targegen, Inc. | Use of bi-aryl meta-pyrimidine inhibitors of kinases |
| MY167260A (en) * | 2005-11-01 | 2018-08-14 | Targegen Inc | Bi-aryl meta-pyrimidine inhibitors of kinases |
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| US7834024B2 (en) * | 2007-03-26 | 2010-11-16 | Rigel Pharmaceuticals, Inc. | Compositions and methods for inhibition of the JAK pathway |
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