JP2009519979A5 - - Google Patents
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- Publication number
- JP2009519979A5 JP2009519979A5 JP2008545992A JP2008545992A JP2009519979A5 JP 2009519979 A5 JP2009519979 A5 JP 2009519979A5 JP 2008545992 A JP2008545992 A JP 2008545992A JP 2008545992 A JP2008545992 A JP 2008545992A JP 2009519979 A5 JP2009519979 A5 JP 2009519979A5
- Authority
- JP
- Japan
- Prior art keywords
- exo
- hept
- diamine
- racemic
- phenyl
- 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
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- -1 -C 1 -C 6 haloalkyl Chemical group 0.000 claims 77
- 150000001875 compounds Chemical class 0.000 claims 24
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 14
- 125000000217 alkyl group Chemical group 0.000 claims 9
- PFXXTYUSZRFQHC-UHFFFAOYSA-N 2-methylhept-5-enamide Chemical compound CC=CCCC(C)C(N)=O PFXXTYUSZRFQHC-UHFFFAOYSA-N 0.000 claims 6
- 125000000753 cycloalkyl group Chemical group 0.000 claims 6
- 229910052736 halogen Inorganic materials 0.000 claims 6
- 150000002367 halogens Chemical class 0.000 claims 6
- 229920006395 saturated elastomer Polymers 0.000 claims 6
- 125000000592 heterocycloalkyl group Chemical group 0.000 claims 5
- 229910052739 hydrogen Inorganic materials 0.000 claims 5
- 239000001257 hydrogen Substances 0.000 claims 5
- 125000004435 hydrogen atom Chemical class [H]* 0.000 claims 5
- 125000004429 atom Chemical group 0.000 claims 4
- 125000000250 methylamino group Chemical group [H]N(*)C([H])([H])[H] 0.000 claims 4
- 125000006413 ring segment Chemical group 0.000 claims 4
- 125000001424 substituent group Chemical group 0.000 claims 4
- QFVJQOMTGRIFGV-UHFFFAOYSA-N 2-imino-1-phenyl-7H-purin-6-amine Chemical compound NC1=NC2=NC=NC2=C(N)N1C1=CC=CC=C1 QFVJQOMTGRIFGV-UHFFFAOYSA-N 0.000 claims 3
- 102000001253 Protein Kinase Human genes 0.000 claims 3
- 125000003710 aryl alkyl group Chemical group 0.000 claims 3
- 125000003118 aryl group Chemical group 0.000 claims 3
- 125000004438 haloalkoxy group Chemical group 0.000 claims 3
- 125000001072 heteroaryl group Chemical group 0.000 claims 3
- 229910052757 nitrogen Inorganic materials 0.000 claims 3
- 108060006633 protein kinase Proteins 0.000 claims 3
- 150000001204 N-oxides Chemical class 0.000 claims 2
- CTZMPBILUBWBEV-UHFFFAOYSA-N NC1=NC(N)=C2C=CN=C2N1C1=CC=CC=C1 Chemical compound NC1=NC(N)=C2C=CN=C2N1C1=CC=CC=C1 CTZMPBILUBWBEV-UHFFFAOYSA-N 0.000 claims 2
- 108091000080 Phosphotransferase Proteins 0.000 claims 2
- 125000003545 alkoxy group Chemical group 0.000 claims 2
- ZTUUVDYQBLRAAC-UHFFFAOYSA-N bicyclo[2.2.1]hept-2-ene-5-carboxamide Chemical compound C1C2C(C(=O)N)CC1C=C2 ZTUUVDYQBLRAAC-UHFFFAOYSA-N 0.000 claims 2
- 150000004985 diamines Chemical class 0.000 claims 2
- 201000010099 disease Diseases 0.000 claims 2
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 2
- 125000001153 fluoro group Chemical group F* 0.000 claims 2
- 230000001404 mediated effect Effects 0.000 claims 2
- 125000004433 nitrogen atom Chemical group N* 0.000 claims 2
- 229910052760 oxygen Inorganic materials 0.000 claims 2
- 102000020233 phosphotransferase Human genes 0.000 claims 2
- 150000003839 salts Chemical class 0.000 claims 2
- 239000012453 solvate Substances 0.000 claims 2
- 229910052717 sulfur Inorganic materials 0.000 claims 2
- GKTQKQTXHNUFSP-UHFFFAOYSA-N thieno[3,4-c]pyrrole-4,6-dione Chemical compound S1C=C2C(=O)NC(=O)C2=C1 GKTQKQTXHNUFSP-UHFFFAOYSA-N 0.000 claims 2
- HGUZNMOMWFNAIA-LYJAMZSYSA-N (1r,3s,4r,5s)-4-[[2-[4-(4-cyclohexylpiperazin-1-yl)anilino]thieno[3,2-d]pyrimidin-4-yl]amino]-n,4,6,6-tetramethylbicyclo[3.1.1]heptane-3-carboxamide Chemical compound N([C@@]1([C@@]2([H])C[C@@](C2(C)C)(C[C@@H]1C(=O)NC)[H])C)C(C=1SC=CC=1N=1)=NC=1NC(C=C1)=CC=C1N(CC1)CCN1C1CCCCC1 HGUZNMOMWFNAIA-LYJAMZSYSA-N 0.000 claims 1
- ZKLXTNAQPVKTED-GUYJKWIASA-N (1s,2s,3r,4r)-3-[[2-(1h-indol-5-ylamino)-7h-purin-6-yl]amino]bicyclo[2.2.1]hept-5-ene-2-carboxamide Chemical compound C1=C2NC=CC2=CC(NC=2NC(=C3N=CN=C3N=2)N[C@H]2[C@H]([C@@]3([H])C[C@@]2(C=C3)[H])C(N)=O)=C1 ZKLXTNAQPVKTED-GUYJKWIASA-N 0.000 claims 1
- BCCAFVDIHPOCSV-LCLWPZTBSA-N (1s,2s,3r,4r)-3-[[2-[4-(pyridin-4-ylmethyl)anilino]-7h-purin-6-yl]amino]bicyclo[2.2.1]hept-5-ene-2-carboxamide Chemical compound N([C@H]1[C@H]([C@@]2([H])C[C@@]1(C=C2)[H])C(N)=O)C(=C1N=CN=C1N=1)NC=1NC(C=C1)=CC=C1CC1=CC=NC=C1 BCCAFVDIHPOCSV-LCLWPZTBSA-N 0.000 claims 1
- 125000006552 (C3-C8) cycloalkyl group Chemical group 0.000 claims 1
- 125000005809 3,4,5-trimethoxyphenyl group Chemical group [H]C1=C(OC([H])([H])[H])C(OC([H])([H])[H])=C(OC([H])([H])[H])C([H])=C1* 0.000 claims 1
- CSPKGUCKMUMGIG-UHFFFAOYSA-N 6-phenylthieno[3,2-d]pyrimidine-2,4-diamine Chemical compound C=1C2=NC(N)=NC(N)=C2SC=1C1=CC=CC=C1 CSPKGUCKMUMGIG-UHFFFAOYSA-N 0.000 claims 1
- 125000005915 C6-C14 aryl group Chemical group 0.000 claims 1
- TZGDXHITFVTUJO-UHFFFAOYSA-N CC(C=C(C=C1)C2=C3C(N)=NC(N)=NC3=CC=C2)=C1OCCN1CCCC1 Chemical compound CC(C=C(C=C1)C2=C3C(N)=NC(N)=NC3=CC=C2)=C1OCCN1CCCC1 TZGDXHITFVTUJO-UHFFFAOYSA-N 0.000 claims 1
- 102000000551 Syk Kinase Human genes 0.000 claims 1
- 108010016672 Syk Kinase Proteins 0.000 claims 1
- 125000002947 alkylene group Chemical group 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
- 125000004432 carbon atom Chemical group C* 0.000 claims 1
- 150000003857 carboxamides Chemical class 0.000 claims 1
- 239000003085 diluting agent Substances 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 230000000694 effects Effects 0.000 claims 1
- 125000001188 haloalkyl group Chemical group 0.000 claims 1
- 125000005843 halogen group Chemical group 0.000 claims 1
- 125000004474 heteroalkylene group Chemical group 0.000 claims 1
- 125000004446 heteroarylalkyl group Chemical group 0.000 claims 1
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 1
- 125000002768 hydroxyalkyl group Chemical group 0.000 claims 1
- 230000002401 inhibitory effect Effects 0.000 claims 1
- 230000005764 inhibitory process Effects 0.000 claims 1
- 239000000546 pharmaceutical excipient Substances 0.000 claims 1
- 125000002924 primary amino group Chemical group [H]N([H])* 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
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 claims 1
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 claims 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US75139305P | 2005-12-15 | 2005-12-15 | |
| US60/751,393 | 2005-12-15 | ||
| PCT/US2006/062162 WO2007070872A1 (en) | 2005-12-15 | 2006-12-15 | Kinase inhibitors and their uses |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2009519979A JP2009519979A (ja) | 2009-05-21 |
| JP2009519979A5 true JP2009519979A5 (enExample) | 2010-02-04 |
| JP5400388B2 JP5400388B2 (ja) | 2014-01-29 |
Family
ID=37891850
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2008545992A Expired - Fee Related JP5400388B2 (ja) | 2005-12-15 | 2006-12-15 | キナーゼインヒビターおよびその利用 |
Country Status (6)
| Country | Link |
|---|---|
| US (4) | US7601713B2 (enExample) |
| EP (1) | EP1960372B1 (enExample) |
| JP (1) | JP5400388B2 (enExample) |
| CA (1) | CA2633035C (enExample) |
| ES (1) | ES2562428T3 (enExample) |
| WO (1) | WO2007070872A1 (enExample) |
Families Citing this family (79)
| Publication number | Priority date | Publication date | Assignee | Title |
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| WO2007070872A1 (en) * | 2005-12-15 | 2007-06-21 | Rigel Pharmaceuticals, Inc. | Kinase inhibitors and their uses |
| TW201336514A (zh) * | 2006-04-13 | 2013-09-16 | Alcon Res Ltd | ＲＮＡ干擾（ＲＮＡｉ）所媒介之與脾酪胺酸激酶相關之發炎症狀的抑制作用（二） |
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| GEP20125691B (en) | 2006-12-08 | 2012-11-26 | Irm Llc | Compounds and compositions as protein kinase inhibitors |
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| EP2170395A1 (en) * | 2007-07-02 | 2010-04-07 | Wyeth LLC | Modulators of axl for use in treating bone disorders |
| RU2472797C2 (ru) * | 2007-08-08 | 2013-01-20 | ГЛАКСОСМИТКЛАЙН ЭлЭлСи | ПРОИЗВОДНЫЕ 2-[(2-(ФЕНИЛАМИНО)-1Н-ПИРРОЛО[2,3-d]ПИРИМИДИН-4-ИЛ)АМИНО]БЕНЗАМИДА В КАЧЕСТВЕ ИНГИБИТОРОВ IGF-1R ДЛЯ ЛЕЧЕНИЯ РАКА |
| WO2009032694A1 (en) * | 2007-08-28 | 2009-03-12 | Dana Farber Cancer Institute | Amino substituted pyrimidine, pyrollopyridine and pyrazolopyrimidine derivatives useful as kinase inhibitors and in treating proliferative disorders and diseases associated with angiogenesis |
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| EP2219671A4 (en) | 2007-11-09 | 2011-02-09 | Salk Inst For Biological Studi | USE OF TAM RECEPTOR INHIBITORS AS IMMU ENHANCERS AND TAM ACTIVATORS AS IMMUNOSUPPRESSORS |
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| TW200942537A (en) * | 2008-02-01 | 2009-10-16 | Irm Llc | Compounds and compositions as kinase 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 |
| WO2009131687A2 (en) * | 2008-04-22 | 2009-10-29 | Portola Pharmaceuticals, Inc. | Inhibitors of protein kinases |
| EP2296475A4 (en) | 2008-06-20 | 2014-03-05 | Genentech Inc | TRIAZOLOPYRIDINE COMPOUNDS JAK KINASE INHIBITORS AND METHODS |
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| CA2749843C (en) | 2009-01-16 | 2017-09-05 | Rigel Pharmaceuticals, Inc. | Axl inhibitors for use in combination therapy for preventing, treating or managing metastatic cancer |
| TW201041892A (en) * | 2009-02-09 | 2010-12-01 | Supergen Inc | Pyrrolopyrimidinyl Axl kinase inhibitors |
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| TW201105669A (en) * | 2009-07-30 | 2011-02-16 | Irm Llc | Compounds and compositions as Syk kinase inhibitors |
| WO2011014795A2 (en) | 2009-07-30 | 2011-02-03 | Irm Llc | Compounds and compositions as syk kinase inhibitors |
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| WO2013052393A1 (en) | 2011-10-05 | 2013-04-11 | Merck Sharp & Dohme Corp. | 3-PYRIDYL CARBOXAMIDE-CONTAINING SPLEEN TYROSINE KINASE (Syk) INHIBITORS |
| WO2013052394A1 (en) | 2011-10-05 | 2013-04-11 | Merck Sharp & Dohme Corp. | 2-pyridyl carboxamide-containing spleen tyrosine kinase (syk) inhibitors |
| WO2013052391A1 (en) | 2011-10-05 | 2013-04-11 | Merck Sharp & Dohme Corp. | PHENYL CARBOXAMIDE-CONTAINING SPLEEN TYROSINE KINASE (Syk) INHIBITORS |
| JP6039683B2 (ja) | 2011-11-23 | 2016-12-07 | ポートラ ファーマシューティカルズ， インコーポレイテッド | ピラジンキナーゼ阻害剤 |
| SG11201404505PA (en) | 2012-01-31 | 2014-10-30 | Daiichi Sankyo Co Ltd | Pyridone derivative |
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| US9487504B2 (en) | 2012-06-20 | 2016-11-08 | Merck Sharp & Dohme Corp. | Imidazolyl analogs as syk inhibitors |
| US9416111B2 (en) | 2012-06-22 | 2016-08-16 | Merck Sharp & Dohme Corp. | Substituted diazine and triazine spleen tyrosine kinease (Syk) inhibitors |
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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 |
| EP3184121A3 (en) | 2012-07-25 | 2017-09-27 | Salk Institute For Biological Studies | Lipid membranes with exposed phosphatidylserine as tam ligands, use for treating autoimmune diseases |
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| EP2988744A4 (en) | 2013-04-26 | 2016-11-02 | Merck Sharp & Dohme | THIAZOLSUBSTITUTED AMINOHETEROARYLE AS MILZTYROSINKINASE INHIBITOR |
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| WO2015138273A1 (en) | 2014-03-13 | 2015-09-17 | Merck Sharp & Dohme Corp. | 2-pyrazine carboxamides as spleen tyrosine kinase inhibitors |
| TWI723572B (zh) | 2014-07-07 | 2021-04-01 | 日商第一三共股份有限公司 | 具有四氫吡喃基甲基之吡啶酮衍生物及其用途 |
| WO2016073771A2 (en) * | 2014-11-06 | 2016-05-12 | Ohio State Innovation Foundation | Pyrrolopyrimidine derivatives as mps1/ttk kinase inhibitors |
| PL3233857T3 (pl) * | 2014-12-18 | 2020-07-27 | Takeda Pharmaceutical Company Limited | Stałe postacie skondensowanych heteroaromatycznych pirolidynonów |
| US9840503B2 (en) | 2015-05-11 | 2017-12-12 | Incyte Corporation | Heterocyclic compounds and uses thereof |
| US9708333B2 (en) | 2015-08-12 | 2017-07-18 | Incyte Corporation | Fused bicyclic 1,2,4-triazine compounds as TAM inhibitors |
| WO2017035366A1 (en) | 2015-08-26 | 2017-03-02 | Incyte Corporation | Pyrrolopyrimidine derivatives as tam inhibitors |
| EP3421039B1 (en) | 2016-02-26 | 2021-10-06 | ONO Pharmaceutical Co., Ltd. | Drug for cancer therapy characterized by administering combination between axl inhibitor and immune checkpoint inhibitor |
| PT3436461T (pt) | 2016-03-28 | 2024-01-23 | Incyte Corp | Compostos de pirrolotriazina como inibidores de tam |
| CN107698603B (zh) | 2016-08-09 | 2022-04-08 | 南京红云生物科技有限公司 | 噻吩并嘧啶类化合物、其制备方法、药用组合物及其应用 |
| 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 |
| JP7156287B2 (ja) | 2017-08-23 | 2022-10-19 | 小野薬品工業株式会社 | Ａｘｌ阻害剤を有効成分として含むがん治療剤 |
| US10633387B2 (en) | 2017-09-27 | 2020-04-28 | Incyte Corporation | Salts of TAM inhibitors |
| EP3695839A4 (en) | 2017-10-13 | 2021-07-14 | ONO Pharmaceutical Co., Ltd. | THERAPEUTIC AGENT WITH AXL INHIBITOR AS AN ACTIVE INGREDIENT FOR SOLID TUMORS |
| US12012408B2 (en) | 2018-06-22 | 2024-06-18 | The Royal Institution For The Advancement Of Learning/Mcgill University | Purine compounds and method for the treatment of cancer |
| SI3813800T1 (sl) | 2018-06-29 | 2025-07-31 | Incyte Corporation | Formulacije zaviralca axl/mer |
| EP3947737A2 (en) | 2019-04-02 | 2022-02-09 | 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 |
| JP2023516441A (ja) | 2020-03-06 | 2023-04-19 | インサイト・コーポレイション | Ａｘｌ／ｍｅｒ阻害剤及びｐｄ－１／ｐｄ－ｌ１阻害剤を含む併用療法 |
| US20250283174A1 (en) | 2022-05-16 | 2025-09-11 | Institut National de la Santé et de la Recherche Médicale | Methods for assessing the exhaustion of hematopoietic stem cells induced by chronic inflammation |
| WO2024054793A1 (en) | 2022-09-09 | 2024-03-14 | University Of Rochester | Inhibition of efferocytosis as a treatment to prevent bone loss and increase bone density and strength |
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| US6897307B2 (en) * | 2002-03-28 | 2005-05-24 | Novartis Ag | Process for preparing 2,6-diaminopurine derivatives |
| US7129239B2 (en) | 2002-10-28 | 2006-10-31 | Pfizer Inc. | Purine compounds and uses thereof |
| WO2004043367A2 (en) * | 2002-11-06 | 2004-05-27 | Bristol-Myers Squibb Company | Fused heterocyclic compounds and use thereof |
| ES2349534T3 (es) | 2003-07-14 | 2011-01-04 | University Of Limerick | Injerto vascular. |
| US20050124637A1 (en) * | 2003-08-15 | 2005-06-09 | Irm Llc | Compounds and compositions as inhibitors of receptor tyrosine kinase activity |
| ES2398239T3 (es) | 2003-11-10 | 2013-03-14 | The Scripps Research Institute | Composiciones y procedimientos para inducir la desdiferenciación celular |
| GB0327319D0 (en) | 2003-11-24 | 2003-12-24 | Pfizer Ltd | Novel pharmaceuticals |
| SI1697356T1 (sl) * | 2003-12-16 | 2008-06-30 | Pfizer Prod Inc | Pirido(2,3-d)pirimidin-2,4-diamini kot zaviralci PDE 2 |
| GB0407723D0 (en) | 2004-04-05 | 2004-05-12 | Novartis Ag | Organic compounds |
| 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 |
| US20060025406A1 (en) * | 2004-07-06 | 2006-02-02 | Angion Biomedica Corporation | Modulators of hepatocyte growth factor/c- Met activity |
| WO2006055528A2 (en) | 2004-11-15 | 2006-05-26 | Rigel Pharmaceuticals, Inc. | Process for the preparation of an optically acitive n-carbamate protected beta-lactam by optical resolution employing a candida antarctica lipase |
| GB2420559B (en) | 2004-11-15 | 2008-08-06 | Rigel Pharmaceuticals Inc | Stereoisomerically enriched 3-aminocarbonyl bicycloheptene pyrimidinediamine compounds and their uses |
| WO2006105056A2 (en) * | 2005-03-28 | 2006-10-05 | Fmc Corporation | Insecticidal 2,4-diaminoquinazolines and related derivatives |
| CN100526315C (zh) * | 2005-06-16 | 2009-08-12 | 浙江医药股份有限公司新昌制药厂 | N2-喹啉或异喹啉取代的嘌呤衍生物及其制备方法和其用途 |
| WO2007042298A1 (en) | 2005-10-13 | 2007-04-19 | Glaxo Group Limited | Pyrrolopyrimidine derivatives as syk inhibitors |
| WO2007070872A1 (en) * | 2005-12-15 | 2007-06-21 | Rigel Pharmaceuticals, Inc. | Kinase inhibitors and their uses |
-
2006
- 2006-12-15 WO PCT/US2006/062162 patent/WO2007070872A1/en not_active Ceased
- 2006-12-15 EP EP06840283.3A patent/EP1960372B1/en not_active Not-in-force
- 2006-12-15 US US11/611,568 patent/US7601713B2/en active Active
- 2006-12-15 CA CA2633035A patent/CA2633035C/en active Active
- 2006-12-15 ES ES06840283.3T patent/ES2562428T3/es active Active
- 2006-12-15 JP JP2008545992A patent/JP5400388B2/ja not_active Expired - Fee Related
-
2009
- 2009-09-01 US US12/552,125 patent/US8053434B2/en active Active
-
2011
- 2011-09-23 US US13/242,994 patent/US9096542B2/en active Active
-
2015
- 2015-06-30 US US14/754,989 patent/US9834568B2/en active Active
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