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 (85)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US6638926B2 (en) * | 2000-09-15 | 2003-10-28 | 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 |
| US8178671B2 (en) | 2003-07-30 | 2012-05-15 | Rigel Pharmaceuticals, Inc. | Methods of treating or preventing autoimmune diseases with 2, 4-pyrimidinediamine compounds |
| RU2007107177A (ru) * | 2004-07-28 | 2008-09-10 | Айрм Ллк (Bm) | Соединения и композиции, как модуляторы ядерных рецепторов стероидных гормонов |
| WO2006047492A2 (en) | 2004-10-22 | 2006-05-04 | Amgen Inc. | Substituted nitrogen-containing heterocycles as vanilloid receptor ligands and their uses as medicament |
| EP1814878B1 (en) | 2004-11-24 | 2012-01-04 | Rigel Pharmaceuticals, Inc. | Spiro-2, 4-pyrimidinediamine compounds and their uses |
| JP5154231B2 (ja) * | 2005-02-14 | 2013-02-27 | ジョンソン・アンド・ジョンソン・ビジョン・ケア・インコーポレイテッド | 快適な眼科用具およびその製造法 |
| CA2604551A1 (en) * | 2005-05-03 | 2007-03-08 | Rigel Pharmaceuticals, Inc. | Jak kinase inhibitors and their uses |
| CN105348203B (zh) | 2005-06-08 | 2018-09-18 | 里格尔药品股份有限公司 | 抑制jak途径的组合物和方法 |
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| US8604042B2 (en) | 2005-11-01 | 2013-12-10 | Targegen, Inc. | Bi-aryl meta-pyrimidine inhibitors of kinases |
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| 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 |
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| WO2014013014A1 (en) | 2012-07-18 | 2014-01-23 | Fundació Privada Centre De Regulació Genòmica (Crg) | Jak inhibitors for activation of epidermal stem cell populations |
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| HUE041877T2 (hu) | 2013-10-17 | 2019-06-28 | Vertex Pharma | (S)-N-Metil-8-(1-((2'-metil-[4,5'-bipirimidin]-6-il)amino)propán-2-il)kinolin-4-karboxamid kokristályai és deuterált származékai DNS-PK inhibitorokként |
| 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 |
| TWI729644B (zh) | 2014-06-12 | 2021-06-01 | 美商西爾拉癌症醫學公司 | N-(氰基甲基)-4-(2-(4-𠰌啉基苯基胺基)嘧啶-4-基)苯甲醯胺 |
| TWI704151B (zh) * | 2014-12-22 | 2020-09-11 | 美商美國禮來大藥廠 | Ｅｒｋ抑制劑 |
| GB201509893D0 (en) * | 2015-06-08 | 2015-07-22 | Ucb Biopharma Sprl | Therapeutic agents |
| 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 |
| US11110108B2 (en) | 2016-09-27 | 2021-09-07 | Vertex Pharmaceuticals Incorporated | Method for treating cancer using a combination of DNA-damaging agents and DNA-PK inhibitors |
| WO2019113487A1 (en) | 2017-12-08 | 2019-06-13 | Incyte Corporation | Low dose combination therapy for treatment of myeloproliferative neoplasms |
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| GB9523675D0 (en) | 1995-11-20 | 1996-01-24 | Celltech Therapeutics Ltd | Chemical compounds |
| RU2277911C2 (ru) * | 2000-02-25 | 2006-06-20 | Ф.Хоффманн-Ля Рош Аг | Модуляторы аденозиновых рецепторов |
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| CA2441733A1 (en) * | 2001-03-29 | 2002-10-10 | Vertex Pharmaceuticals Incorporated | Inhibitors of c-jun n-terminal kinases (jnk) and other protein kinases |
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2003
- 2003-11-04 AT AT03786582T patent/ATE371656T1/de not_active IP Right Cessation
- 2003-11-04 US US10/700,936 patent/US7259161B2/en not_active Expired - Fee Related
- 2003-11-04 WO PCT/US2003/035163 patent/WO2004041814A1/en not_active Ceased
- 2003-11-04 DE DE60316013T patent/DE60316013T2/de not_active Expired - Lifetime
- 2003-11-04 JP JP2004550483A patent/JP4688498B2/ja not_active Expired - Fee Related
- 2003-11-04 AU AU2003295396A patent/AU2003295396B2/en not_active Ceased
- 2003-11-04 ES ES03786582T patent/ES2289349T3/es not_active Expired - Lifetime
- 2003-11-04 CA CA002506773A patent/CA2506773A1/en not_active Abandoned
- 2003-11-04 EP EP03786582A patent/EP1562938B1/en not_active Expired - Lifetime
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2010
- 2010-09-21 JP JP2010211038A patent/JP2011016839A/ja active Pending