JP2009519979A5 - - Google Patents
Download PDFInfo
- 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
Links
- -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 (https=) | 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 (https=) |
| EP (1) | EP1960372B1 (https=) |
| JP (1) | JP5400388B2 (https=) |
| CA (1) | CA2633035C (https=) |
| ES (1) | ES2562428T3 (https=) |
| WO (1) | WO2007070872A1 (https=) |
Families Citing this family (79)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| MX2007013595A (es) | 2005-05-04 | 2008-01-24 | Renovis Inc | Compuestos heterociclicos fusionados y composiciones y usos de estos. |
| JP5400388B2 (ja) * | 2005-12-15 | 2014-01-29 | 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 | キナーゼインヒビターおよびその利用 |
| TW200808360A (en) * | 2006-04-13 | 2008-02-16 | Alcon Mfg Ltd | RNAi-mediated inhibition of spleen tyrosine kinase-related inflammatory conditions |
| WO2008045978A1 (en) * | 2006-10-10 | 2008-04-17 | Rigel Pharmaceuticals, Inc. | Pinane-substituted pyrimidinediamine derivatives useful as axl inhibitors |
| EP2311807B1 (en) | 2006-12-08 | 2015-11-11 | Novartis AG | Compounds and composition as protein kinase inhibitors |
| US20100298557A1 (en) | 2006-12-28 | 2010-11-25 | Taisho Pharmaceutical Co., Ltd | Pyrazolopyrimidine compound |
| WO2009005813A1 (en) * | 2007-07-02 | 2009-01-08 | Wyeth | Modulators of axl for use in treating bone disorders |
| US7981903B2 (en) * | 2007-08-08 | 2011-07-19 | Glaxosmithkline Llc | 2-[2-{phenylamino}-1H-pyrrolo[2,3-D]pyrimidin-4-yl)amino] benzamide derivatives as IGF-1R inhibitors for the treatment of cancer |
| WO2009032703A1 (en) * | 2007-08-28 | 2009-03-12 | Irm Llc | 2- (het) arylamino-6-aminopyridine derivatives and fused forms thereof as anaplastic lymphoma kinase inhibitors |
| WO2009029682A1 (en) * | 2007-08-28 | 2009-03-05 | Rigel Pharmaceuticals, Inc. | Combination therapy with syk kinase inhibitor |
| EP2217716A4 (en) | 2007-11-09 | 2011-02-09 | Salk Inst For Biological Studi | USE OF TAM RECEPTOR INHIBITORS AS ANTIMICROBIAL AGENTS |
| EP3109249A1 (en) | 2007-11-15 | 2016-12-28 | YM BioSciences Australia Pty Ltd | N-containing heterocyclic compounds |
| TW200942537A (en) * | 2008-02-01 | 2009-10-16 | Irm Llc | Compounds and compositions as kinase inhibitors |
| MX2010011463A (es) | 2008-04-16 | 2011-06-03 | Portola Pharm Inc | 2,6-diamino-pirimidin-5-il-carboxamidas como inhibidores de syk o jak quinasas. |
| US8138339B2 (en) | 2008-04-16 | 2012-03-20 | Portola Pharmaceuticals, Inc. | Inhibitors of protein kinases |
| NZ588830A (en) * | 2008-04-22 | 2012-11-30 | Portola Pharm Inc | Inhibitors of protein kinases |
| BRPI0909945A2 (pt) | 2008-06-20 | 2015-07-28 | Genentech Inc | "composto, composição farmacêutica, método para tratar ou atenuar a gravidade de uma doença ou condição responsiva à inibição da atividade jak2 quinase em um paciente, kit para o tratamento de uma doença ou distúrbio responsivo à inibição da jak quinase" |
| EP2288260A4 (en) | 2008-06-20 | 2013-10-23 | Genentech Inc | TRIAZOLOPYRIDINE-JAK HEMMER COMPOUNDS AND METHOD |
| SG172997A1 (en) | 2009-01-16 | 2011-08-29 | Rigel Pharmaceuticals Inc | Axl inhibitors for use in combination therapy for preventing, treating or managing metastatic cancer |
| US20100204221A1 (en) * | 2009-02-09 | 2010-08-12 | Hariprasad Vankayalapati | Pyrrolopyrimidinyl axl kinase inhibitors |
| TW201100427A (en) | 2009-03-31 | 2011-01-01 | Arqule Inc | Substituted heterocyclic compounds |
| CN105037364B (zh) * | 2009-04-03 | 2018-04-27 | 维拉斯通股份有限公司 | 作为激酶抑制剂的嘧啶取代的嘌呤化合物 |
| ES2500643T3 (es) | 2009-04-03 | 2014-09-30 | Verastem, Inc. | Compuestos de purina sustituidos con pirimidina como inhibidores de las cinasas |
| TW201105669A (en) * | 2009-07-30 | 2011-02-16 | Irm Llc | Compounds and compositions as Syk kinase inhibitors |
| JP2013501002A (ja) | 2009-07-30 | 2013-01-10 | アイアールエム・リミテッド・ライアビリティ・カンパニー | Ｓｙｋキナーゼ阻害剤としての化合物および組成物 |
| CN102471338B (zh) | 2009-08-07 | 2014-07-02 | 默克专利有限公司 | 氮杂杂环化合物 |
| KR101094446B1 (ko) | 2009-11-19 | 2011-12-15 | 한국과학기술연구원 | 단백질 키나아제 저해활성을 가지는 2,4,7-치환된 티에노［3,2-ｄ］피리미딘 화합물 |
| SG181857A1 (en) * | 2009-12-23 | 2012-07-30 | Takeda Pharmaceutical | Fused heteroaromatic pyrrolidinones as syk inhibitors |
| EP2441755A1 (en) * | 2010-09-30 | 2012-04-18 | Almirall, S.A. | Pyridine- and isoquinoline-derivatives as Syk and JAK kinase inhibitors |
| FR2967854A1 (fr) * | 2010-11-19 | 2012-05-25 | France Telecom | Procede de communication dans un reseau cooperatif |
| EP2489663A1 (en) | 2011-02-16 | 2012-08-22 | Almirall, S.A. | Compounds as syk kinase inhibitors |
| MX343517B (es) | 2011-03-10 | 2016-11-07 | Rigel Pharmaceuticals Inc | 2,4 pirimidinadiaminas sustituidas para su uso en lupus discoide. |
| EP2707357B1 (en) | 2011-05-10 | 2017-01-18 | Merck Sharp & Dohme Corp. | Pyridyl aminopyridines as syk inhibitors |
| US9145391B2 (en) | 2011-05-10 | 2015-09-29 | Merck Sharp & Dohme Corp. | Bipyridylaminopyridines as Syk inhibitors |
| MX2013013090A (es) | 2011-05-10 | 2013-12-16 | Merck Sharp & Dohme | Aminopirimidinas como inhibidores de tirosina cinaza del bazo. |
| JP6026525B2 (ja) * | 2011-06-22 | 2016-11-16 | 武田薬品工業株式会社 | 置換６−アザ−イソインドリン−１−オン誘導体 |
| WO2013052391A1 (en) | 2011-10-05 | 2013-04-11 | Merck Sharp & Dohme Corp. | PHENYL CARBOXAMIDE-CONTAINING SPLEEN TYROSINE KINASE (Syk) INHIBITORS |
| EP2763976B1 (en) | 2011-10-05 | 2016-05-18 | Merck Sharp & Dohme Corp. | 2-pyridyl carboxamide-containing spleen tyrosine kinase (syk) inhibitors |
| WO2013052393A1 (en) | 2011-10-05 | 2013-04-11 | Merck Sharp & Dohme Corp. | 3-PYRIDYL CARBOXAMIDE-CONTAINING SPLEEN TYROSINE KINASE (Syk) INHIBITORS |
| CA3094793A1 (en) | 2011-11-23 | 2013-05-30 | Portola Pharmaceuticals, Inc. | Pyrazine kinase inhibitors |
| RS55728B1 (sr) | 2012-01-31 | 2017-07-31 | Daiichi Sankyo Co Ltd | Derivat piridona |
| WO2013162061A1 (ja) * | 2012-04-26 | 2013-10-31 | 第一三共株式会社 | 二環性ピリミジン化合物 |
| US9487504B2 (en) | 2012-06-20 | 2016-11-08 | Merck Sharp & Dohme Corp. | Imidazolyl analogs as syk inhibitors |
| EP2863914B1 (en) | 2012-06-20 | 2018-10-03 | Merck Sharp & Dohme Corp. | Pyrazolyl derivatives as syk inhibitors |
| EP2863915B1 (en) | 2012-06-22 | 2017-12-06 | Merck Sharp & Dohme Corp. | SUBSTITUTED DIAZINE AND TRIAZINE SPLEEN TYROSINE KINASE (Syk) INHIBITORS |
| EP2863916B1 (en) | 2012-06-22 | 2018-07-18 | Merck Sharp & Dohme Corp. | Substituted pyridine spleen tyrosine kinase (syk) inhibitors |
| WO2014013014A1 (en) | 2012-07-18 | 2014-01-23 | Fundació Privada Centre De Regulació Genòmica (Crg) | Jak inhibitors for activation of epidermal stem cell populations |
| CA2879542A1 (en) | 2012-07-25 | 2014-01-30 | Salk Institute For Biological Studies | Regulating the interaction between tam ligands and lipid membranes with exposed phosphatidylserine |
| EP2884982B1 (en) | 2012-08-20 | 2017-09-20 | Merck Sharp & Dohme Corp. | SUBSTITUTED PHENYL SPLEEN TYROSINE KINASE (Syk) INHIBITORS |
| EP2895172B1 (en) | 2012-09-12 | 2019-02-06 | Rigel Pharmaceuticals, Inc. | Treatment for vitiligo |
| EP2900665B1 (en) | 2012-09-28 | 2018-01-03 | Merck Sharp & Dohme Corp. | Triazolyl derivatives as syk inhibitors |
| WO2014093191A1 (en) | 2012-12-12 | 2014-06-19 | Merck Sharp & Dohme Corp. | AMINO-PYRIMIDINE-CONTAINING SPLEEN TYROSINE KINASE (Syk) INHIBITORS |
| EP2934525B1 (en) | 2012-12-21 | 2019-05-08 | Merck Sharp & Dohme Corp. | Thiazole-substituted aminopyridines as spleen tyrosine kinase inhibitors |
| EP2988744A4 (en) | 2013-04-26 | 2016-11-02 | Merck Sharp & Dohme | THIAZOLSUBSTITUTED AMINOHETEROARYLE AS MILZTYROSINKINASE INHIBITOR |
| EP2988749B1 (en) | 2013-04-26 | 2019-08-14 | Merck Sharp & Dohme Corp. | Thiazole-substituted aminopyrimidines as spleen tyrosine kinase inhibitors |
| EP3083560B1 (en) | 2013-12-20 | 2021-10-27 | Merck Sharp & Dohme Corp. | Thiazole-substituted aminoheteroaryls as spleen tyrosine kinase inhibitors |
| US9822107B2 (en) | 2013-12-20 | 2017-11-21 | Merck Sharp & Dohme Corp. | Thiazole-substituted aminoheteroaryls as spleen tyrosine kinase inhibitors |
| US9783531B2 (en) | 2013-12-20 | 2017-10-10 | Merck Sharp & Dohme Corp. | Thiazole-substituted aminoheteroaryls as spleen tyrosine kinase inhibitors |
| WO2015138273A1 (en) | 2014-03-13 | 2015-09-17 | Merck Sharp & Dohme Corp. | 2-pyrazine carboxamides as spleen tyrosine kinase inhibitors |
| TWI690525B (zh) | 2014-07-07 | 2020-04-11 | 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 |
| US10611765B2 (en) | 2014-11-06 | 2020-04-07 | Ohio State Innovation Foundation | Pyrrolopyrimidine derivatives as Mps1/TTK kinase inhibitors |
| MY199935A (en) * | 2014-12-18 | 2023-11-29 | Wells Therapeutics Inc | Solid state forms of fused heteroaromatic pyrrolidinones |
| US9840503B2 (en) | 2015-05-11 | 2017-12-12 | Incyte Corporation | Heterocyclic compounds and uses thereof |
| WO2017027717A1 (en) | 2015-08-12 | 2017-02-16 | Incyte Corporation | Bicyclic fused pyrimidine compounds as tam inhibitors |
| US10053465B2 (en) | 2015-08-26 | 2018-08-21 | Incyte Corporation | Pyrrolopyrimidine derivatives as TAM inhibitors |
| WO2017146236A1 (ja) | 2016-02-26 | 2017-08-31 | 小野薬品工業株式会社 | Ａｘｌ阻害剤と免疫チェックポイント阻害剤とを組み合わせて投与することを特徴とする癌治療のための医薬 |
| MD3436461T2 (ro) | 2016-03-28 | 2024-05-31 | Incyte Corp | Compuși pirolotriazină ca inhibitori 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 |
| SI3687996T1 (sl) | 2017-09-27 | 2022-04-29 | Incyte Corporation | Soli pirolotriazinskih derivatov, ki so uporabne kot zaviralci TAM |
| EP3695839A4 (en) | 2017-10-13 | 2021-07-14 | ONO Pharmaceutical Co., Ltd. | THERAPEUTIC AGENT WITH AXL INHIBITOR AS AN ACTIVE INGREDIENT FOR SOLID TUMORS |
| EP3814354B1 (en) * | 2018-06-22 | 2023-11-08 | The Royal Institution for the Advancement of Learning / McGill University | Purine compounds and method for the treatment of cancer |
| MD3813800T2 (ro) | 2018-06-29 | 2025-10-31 | Incyte Corp | Formulări de inhibitor al AXL/MER |
| JP2022527972A (ja) | 2019-04-02 | 2022-06-07 | アンスティチュ ナショナル ドゥ ラ サンテ エ ドゥ ラ ルシェルシュ メディカル | 前悪性病変を有する患者において癌を予測及び予防する方法 |
| US20220202820A1 (en) | 2019-04-16 | 2022-06-30 | 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 |
| EP4114401A1 (en) | 2020-03-06 | 2023-01-11 | Incyte Corporation | Combination therapy comprising axl/mer and pd-1/pd-l1 inhibitors |
| EP4526469A1 (en) | 2022-05-16 | 2025-03-26 | Institut National de la Santé et de la Recherche Médicale | Methods for assessing the exhaustion of hematopoietic stems 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 |
Family Cites Families (27)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| BR9611157A (pt) * | 1995-11-01 | 1999-03-30 | Novartis Ag | Derivados de purina e processos para sua preparação |
| WO1997020822A1 (en) * | 1995-12-01 | 1997-06-12 | Novartis Ag | Quinazolin-2,4-diazirines as npy receptor antagonist |
| AU7692696A (en) * | 1995-12-01 | 1997-06-27 | Novartis Ag | Heteroaryl derivatives |
| GB9903762D0 (en) * | 1999-02-18 | 1999-04-14 | Novartis Ag | Organic compounds |
| GB9918035D0 (en) | 1999-07-30 | 1999-09-29 | Novartis Ag | Organic compounds |
| EP1230225A2 (en) | 1999-11-01 | 2002-08-14 | Eli Lilly And Company | Pharmaceutically active 4-substituted pyrimidine derivatives |
| FR2818642B1 (fr) * | 2000-12-26 | 2005-07-15 | Hoechst Marion Roussel Inc | Nouveaux derives de la purine, leur procede de preparation, leur application a titre de medicaments, compositions pharmaceutiques et nouvelle utilistion |
| PE20030008A1 (es) * | 2001-06-19 | 2003-01-22 | Bristol Myers Squibb Co | Inhibidores duales de pde 7 y pde 4 |
| JP2005509612A (ja) * | 2001-10-12 | 2005-04-14 | アイアールエム エルエルシー | 置換プリンの合成方法 |
| TWI329105B (en) | 2002-02-01 | 2010-08-21 | Rigel Pharmaceuticals Inc | 2,4-pyrimidinediamine compounds and their uses |
| 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 |
| AU2003291310A1 (en) * | 2002-11-06 | 2004-06-03 | Bristol-Myers Squibb Company | Fused heterocyclic compounds and use thereof |
| EP1643936B1 (en) | 2003-07-14 | 2010-08-11 | University of Limerick | A vascular graft |
| EP1656378A4 (en) * | 2003-08-15 | 2011-05-11 | Irm Llc | COMPOUNDS AND COMPOSITIONS INHIBITING TYROSINE KINASE RECEPTOR ACTIVITY |
| US7951592B2 (en) * | 2003-11-10 | 2011-05-31 | The Scripps Research Institute | Compositions and methods for inducing cell dedifferentiation |
| GB0327319D0 (en) | 2003-11-24 | 2003-12-24 | Pfizer Ltd | Novel pharmaceuticals |
| ATE387446T1 (de) * | 2003-12-16 | 2008-03-15 | Pfizer Prod Inc | Pyrido(2,3-d)pyrimidin-2,4-diamine als pde-2- inhibitoren |
| GB0407723D0 (en) * | 2004-04-05 | 2004-05-12 | Novartis Ag | Organic compounds |
| EP1763514A2 (en) | 2004-05-18 | 2007-03-21 | Rigel Pharmaceuticals, Inc. | Cycloalkyl substituted pyrimidinediamine compounds and their uses |
| CN101031551A (zh) * | 2004-07-06 | 2007-09-05 | 安吉永生物制药公司 | 针对癌症治疗的肝细胞生长因子/c－met活性的喹唑啉调节剂 |
| ATE421996T1 (de) | 2004-11-15 | 2009-02-15 | Rigel Pharmaceuticals Inc | Verfahren zur herstellung optisch aktiver n- carbamat-geschützter beta-lactame durch optische auflösung unter verwendung einer 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 |
| JP5400388B2 (ja) * | 2005-12-15 | 2014-01-29 | 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 | キナーゼインヒビターおよびその利用 |
-
2006
- 2006-12-15 JP JP2008545992A patent/JP5400388B2/ja not_active Expired - Fee Related
- 2006-12-15 WO PCT/US2006/062162 patent/WO2007070872A1/en not_active Ceased
- 2006-12-15 ES ES06840283.3T patent/ES2562428T3/es active Active
- 2006-12-15 CA CA2633035A patent/CA2633035C/en active Active
- 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
-
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 not_active Expired - Fee Related
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| JP2009519979A5 (https=) | ||
| JP6754864B2 (ja) | Ｅｇｆｒ変異型キナーゼ活性をモジュレートするための化合物および組成物 | |
| CN103748096B (zh) | 作为蛋白激酶抑制剂的吡咯并嘧啶化合物 | |
| KR101917972B1 (ko) | ERK 억제제로서 티에노[2,3-c]피롤-4-온 유도체 | |
| AU2013300344B2 (en) | N2,N4-bis(4-(piperazine-1-yl)phenyl)pirimidine-2,4-diamine derivative or pharmaceutically acceptable salt thereof, and composition containing same as active ingredient for preventing or treating cancer | |
| Wu et al. | Design and synthesis of tetrahydropyridothieno [2, 3-d] pyrimidine scaffold based epidermal growth factor receptor (EGFR) kinase inhibitors: the role of side chain chirality and Michael acceptor group for maximal potency | |
| AU2010286569B2 (en) | Compounds and compositions as protein kinase inhibitors | |
| US20170224689A1 (en) | Novel pyrrolopyrimidine compounds as inhibitors of protein kinases | |
| FI3932919T3 (fi) | Jak-inhibiittoriyhdiste ja sen käyttö | |
| Dehnhardt et al. | Lead optimization of N-3-substituted 7-morpholinotriazolopyrimidines as dual phosphoinositide 3-kinase/mammalian target of rapamycin inhibitors: discovery of PKI-402 | |
| EA034558B1 (ru) | 4-ИМИДАЗО[1,5-a]ПИРИДАЗИН-1-ИЛ-БЕНЗАМИДЫ В КАЧЕСТВЕ Btk-ИНГИБИТОРОВ | |
| US20190292205A1 (en) | Novel 2,3-Dihydro-1h-imidazo{1,2-a}pyrimidin-5-one and this 1,2,3,4-tetrahydropyrimido{1,2-a}pyrimidin-6-one Derivatives Comprising a Substituted Morpholine, Preparation Thereof and Pharmaceutical Use Thereof | |
| JP2013509438A5 (https=) | ||
| AU2008260772A1 (en) | Novel amide derivative for inhibiting the growth of cancer cells | |
| AU2010267815B2 (en) | Novel 1,2,3,4-tetrahydro-pyrimido(1,2-a)pyrimidin-6-one derivatives, preparation thereof, and pharmaceutical use thereof | |
| WO2015192658A1 (zh) | 一种新型布鲁顿酪氨酸激酶抑制剂 | |
| US20210261554A1 (en) | Ripk2 inhibitors and method of treating cancer with same | |
| ES2627428T3 (es) | Nuevos derivados de 2,3-dihidro-1H-imidazo{1,2-a}pirimidin-5-ona, su preparación y su utilización farmacéutica | |
| WO2021074251A1 (en) | Pyrrolo[2,3-d]pyrimidine derivatives and their use in the treatment of cancer | |
| AU2015274285C1 (en) | Pyrimidine compounds and methods using the same | |
| RU2838180C1 (ru) | Соединения и композиции для модуляции киназной активности мутантов egfr | |
| JP2025536982A (ja) | 改良されたＮＦ－κＢ誘導キナーゼ（ＮＩＫ）阻害剤 | |
| Hamed | Design and synthesis of novel quinazoline-based EGFR kinase inhibitors and dual EGFR/NF-kappa B inhibitors as potential anti-cancer drugs with enhanced efficacy | |
| HK1191936B (en) | Compounds and compositions as protein kinase inhibitors |