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 (86)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DK1318997T3 (da) * | 2000-09-15 | 2006-09-25 | Vertex Pharma | Pyrazolforbindelser der er nyttige som proteinkinase-inhibitorer |
| TWI329105B (en) | 2002-02-01 | 2010-08-21 | Rigel Pharmaceuticals Inc | 2,4-pyrimidinediamine compounds and their uses |
| HRP20050089B1 (hr) | 2002-07-29 | 2015-06-19 | Rigel Pharmaceuticals | Upotreba 2,4 pirimidindiaminskog spoja za proizvodnju lijeka za lijeäśenje ili sprjeäśavanje autoimunosne bolesti |
| JP4886511B2 (ja) | 2003-07-30 | 2012-02-29 | 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 | 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または予防方法 |
| KR20070046150A (ko) * | 2004-07-28 | 2007-05-02 | 아이알엠 엘엘씨 | 스테로이드 호르몬 핵 수용체의 조절제로서의 화합물 및조성물 |
| 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 |
| 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 |
| 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 |
| US20070203161A1 (en) | 2006-02-24 | 2007-08-30 | Rigel Pharmaceuticals, Inc. | Compositions and methods for inhibition of the jak pathway |
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| EP2200436B1 (en) * | 2007-09-04 | 2015-01-21 | The Scripps Research Institute | Substituted pyrimidinyl-amines as protein kinase inhibitors |
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| PL2288610T3 (pl) | 2008-03-11 | 2017-12-29 | Incyte Holdings Corporation | Azetydynowe i cyklobutanowe pochodne jako inhibitory jak |
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| IN2014KN02601A (enExample) | 2012-04-24 | 2015-05-08 | Vertex Pharma | |
| TW201406761A (zh) | 2012-05-18 | 2014-02-16 | Incyte Corp | 做爲ｊａｋ抑制劑之哌啶基環丁基取代之吡咯并吡啶及吡咯并嘧啶衍生物 |
| 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 |
| PL2919766T3 (pl) | 2012-11-15 | 2021-10-04 | Incyte Holdings Corporation | Postacie dawkowania ruksolitynibu o przedłużonym uwalnianiu |
| CN105189509B (zh) | 2013-03-06 | 2017-12-19 | 因赛特公司 | 用于制备jak抑制剂的方法及中间体 |
| SMT202100687T1 (it) | 2013-03-12 | 2022-01-10 | Vertex Pharma | Inibitori della dna-pk |
| SG10201912203XA (en) | 2013-08-07 | 2020-02-27 | Incyte Corp | Sustained release dosage forms for a jak1 inhibitor |
| ES2705342T3 (es) | 2013-10-17 | 2019-03-22 | Vertex Pharma | Co-cristales de (S)-N-metil-8-(1-((2'-metil-[4,5'-bipirimidin]-6-il)amino)propan-2-il)quinolin-4-carboxamida y derivados deuterados de la misma como inhibidores de DNA-PK |
| 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 |
| EP3518931A4 (en) | 2016-09-27 | 2020-05-13 | Vertex Pharmaceuticals Incorporated | METHOD FOR TREATING CANCER WITH A COMBINATION OF DNA-DAMAGING SUBSTANCES AND DNA-PK INHIBITORS |
| WO2019113487A1 (en) | 2017-12-08 | 2019-06-13 | Incyte Corporation | Low dose combination therapy for treatment of myeloproliferative neoplasms |
| EP3746429B1 (en) | 2018-01-30 | 2022-03-09 | Incyte Corporation | Processes for preparing (1-(3-fluoro-2-(trifluoromethyl)isonicotinyl)piperidine-4-one) |
| US11174252B2 (en) * | 2018-02-15 | 2021-11-16 | Nuvation Bio Inc. | Heterocyclic compounds as kinase inhibitors |
| PT3773593T (pt) | 2018-03-30 | 2024-06-25 | Incyte Corp | Tratamento da hidradenite supurativa com inibidores de jak |
| BR112021018168B1 (pt) | 2019-03-21 | 2023-11-28 | Onxeo | Composição farmacêutica, combinação e kit compreendendo uma molécula dbait e um inibidor de quinase para o tratamento de câncer |
| WO2020201362A2 (en) | 2019-04-02 | 2020-10-08 | INSERM (Institut National de la Santé et de la Recherche Médicale) | Methods of predicting and preventing cancer in patients having premalignant lesions |
| WO2020212395A1 (en) | 2019-04-16 | 2020-10-22 | INSERM (Institut National de la Santé et de la Recherche Médicale) | Use of jak inhibitors for the treatment of painful conditions involving nav1.7 channels |
| EP4013753A1 (en) * | 2019-08-14 | 2022-06-22 | Nuvation Bio Inc. | Heterocyclic compounds as kinase inhibitors |
| CA3150689A1 (en) * | 2019-08-14 | 2021-02-18 | Nuvation Bio Inc. | Heterocyclic compounds as kinase inhibitors |
| CA3159348A1 (en) | 2019-11-08 | 2021-05-14 | Inserm (Institut National De La Sante Et De La Recherche Medicale) | Methods for the treatment of cancers that have acquired resistance to kinase inhibitors |
| WO2021148581A1 (en) | 2020-01-22 | 2021-07-29 | Onxeo | Novel dbait molecule and its use |
| US11833155B2 (en) | 2020-06-03 | 2023-12-05 | Incyte Corporation | Combination therapy for treatment of myeloproliferative neoplasms |
| CN115677611B (zh) * | 2021-07-22 | 2024-07-09 | 成都硕德药业有限公司 | 2H-苯并[b][1,4]恶嗪-3(4H）-酮衍生物 |
| CN116947846B (zh) * | 2022-04-15 | 2026-02-27 | 成都硕德药业有限公司 | 一种并环衍生物及其制备方法和用途 |
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Family Cites Families (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| GB9523675D0 (en) * | 1995-11-20 | 1996-01-24 | Celltech Therapeutics Ltd | Chemical compounds |
| KR100521735B1 (ko) * | 2000-02-25 | 2005-10-17 | 에프. 호프만-라 로슈 아게 | 아데노신 수용체 조절인자 |
| WO2002020495A2 (en) * | 2000-09-06 | 2002-03-14 | Chiron Corporation | Inhibitors of glycogen synthase kinase 3 |
| EP1373257B9 (en) * | 2001-03-29 | 2008-10-15 | Vertex Pharmaceuticals Incorporated | Inhibitors of c-jun n-terminal kinases (jnk) and other protein kinases |
| CA2443234A1 (en) | 2001-04-10 | 2002-10-24 | Vertex Pharmaceuticals Incorporated | Isoxaxole derivatives as inhibitors of src and other protein kinases |
| US6825190B2 (en) * | 2001-06-15 | 2004-11-30 | Vertex Pharmaceuticals Incorporated | Protein kinase inhibitors and uses thereof |
-
2003
- 2003-11-04 WO PCT/US2003/035163 patent/WO2004041814A1/en not_active Ceased
- 2003-11-04 US US10/700,936 patent/US7259161B2/en not_active Expired - Fee Related
- 2003-11-04 AT AT03786582T patent/ATE371656T1/de not_active IP Right Cessation
- 2003-11-04 EP EP03786582A patent/EP1562938B1/en not_active Expired - Lifetime
- 2003-11-04 JP JP2004550483A patent/JP4688498B2/ja not_active Expired - Fee Related
- 2003-11-04 CA CA002506773A patent/CA2506773A1/en not_active Abandoned
- 2003-11-04 DE DE60316013T patent/DE60316013T2/de not_active Expired - Lifetime
- 2003-11-04 AU AU2003295396A patent/AU2003295396B2/en not_active Ceased
- 2003-11-04 ES ES03786582T patent/ES2289349T3/es not_active Expired - Lifetime
-
2010
- 2010-09-21 JP JP2010211038A patent/JP2011016839A/ja active Pending
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