JP2008523099A5 - - Google Patents
Download PDFInfo
- Publication number
- JP2008523099A5 JP2008523099A5 JP2007545694A JP2007545694A JP2008523099A5 JP 2008523099 A5 JP2008523099 A5 JP 2008523099A5 JP 2007545694 A JP2007545694 A JP 2007545694A JP 2007545694 A JP2007545694 A JP 2007545694A JP 2008523099 A5 JP2008523099 A5 JP 2008523099A5
- Authority
- JP
- Japan
- Prior art keywords
- alkyl
- aryl
- heteroaryl
- compound
- heteroalkyl
- 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
- 125000003118 aryl group Chemical group 0.000 claims 132
- 125000000217 alkyl group Chemical group 0.000 claims 131
- 125000001072 heteroaryl group Chemical group 0.000 claims 125
- 150000001875 compounds Chemical class 0.000 claims 91
- 229910052739 hydrogen Inorganic materials 0.000 claims 63
- 239000001257 hydrogen Substances 0.000 claims 63
- 125000004404 heteroalkyl group Chemical group 0.000 claims 58
- 150000002431 hydrogen Chemical group 0.000 claims 58
- 125000002252 acyl group Chemical group 0.000 claims 40
- 125000000623 heterocyclic group Chemical group 0.000 claims 35
- 229910052736 halogen Inorganic materials 0.000 claims 26
- 150000002367 halogens Chemical group 0.000 claims 26
- 229910052757 nitrogen Inorganic materials 0.000 claims 21
- 239000003814 drug Substances 0.000 claims 20
- 125000000753 cycloalkyl group Chemical group 0.000 claims 15
- 125000003161 (C1-C6) alkylene group Chemical group 0.000 claims 14
- 125000006590 (C2-C6) alkenylene group Chemical group 0.000 claims 14
- 125000004093 cyano group Chemical group *C#N 0.000 claims 14
- 229940079593 drug Drugs 0.000 claims 13
- 125000000325 methylidene group Chemical group [H]C([H])=* 0.000 claims 13
- -1 heteroaliphatic Chemical group 0.000 claims 11
- 125000004433 nitrogen atom Chemical group N* 0.000 claims 10
- IJGRMHOSHXDMSA-UHFFFAOYSA-N Atomic nitrogen Chemical group N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims 8
- 239000000203 mixture Substances 0.000 claims 7
- 125000002723 alicyclic group Chemical group 0.000 claims 6
- 125000001931 aliphatic group Chemical group 0.000 claims 6
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 6
- 229910052760 oxygen Inorganic materials 0.000 claims 6
- 229910052717 sulfur Inorganic materials 0.000 claims 6
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 5
- 206010028980 Neoplasm Diseases 0.000 claims 5
- 201000011510 cancer Diseases 0.000 claims 5
- 239000003795 chemical substances by application Substances 0.000 claims 5
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 5
- 229910052799 carbon Chemical group 0.000 claims 4
- 125000004432 carbon atom Chemical group C* 0.000 claims 4
- 125000005842 heteroatom Chemical group 0.000 claims 4
- 229940124597 therapeutic agent Drugs 0.000 claims 4
- 208000020084 Bone disease Diseases 0.000 claims 3
- 125000000304 alkynyl group Chemical group 0.000 claims 3
- 208000035475 disorder Diseases 0.000 claims 3
- 125000001188 haloalkyl group Chemical group 0.000 claims 3
- 125000006569 (C5-C6) heterocyclic group Chemical group 0.000 claims 2
- 208000019838 Blood disease Diseases 0.000 claims 2
- 208000024172 Cardiovascular disease Diseases 0.000 claims 2
- 108010025020 Nerve Growth Factor Proteins 0.000 claims 2
- 102000007072 Nerve Growth Factors Human genes 0.000 claims 2
- 125000003342 alkenyl group Chemical group 0.000 claims 2
- 229940124599 anti-inflammatory drug Drugs 0.000 claims 2
- 230000001028 anti-proliverative effect Effects 0.000 claims 2
- 125000000484 butyl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])C([H])([H])[H] 0.000 claims 2
- 230000001066 destructive effect Effects 0.000 claims 2
- 206010012601 diabetes mellitus Diseases 0.000 claims 2
- 201000010099 disease Diseases 0.000 claims 2
- 239000002552 dosage form Substances 0.000 claims 2
- 230000000694 effects Effects 0.000 claims 2
- 208000014951 hematologic disease Diseases 0.000 claims 2
- 208000018706 hematopoietic system disease Diseases 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
- 208000033065 inborn errors of immunity Diseases 0.000 claims 2
- 208000019423 liver disease Diseases 0.000 claims 2
- UHOVQNZJYSORNB-UHFFFAOYSA-N monobenzene Natural products C1=CC=CC=C1 UHOVQNZJYSORNB-UHFFFAOYSA-N 0.000 claims 2
- 239000003900 neurotrophic factor Substances 0.000 claims 2
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 claims 2
- QJGQUHMNIGDVPM-UHFFFAOYSA-N nitrogen group Chemical group [N] QJGQUHMNIGDVPM-UHFFFAOYSA-N 0.000 claims 2
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 2
- 208000028529 primary immunodeficiency disease Diseases 0.000 claims 2
- 230000002062 proliferating effect Effects 0.000 claims 2
- 229920006395 saturated elastomer Polymers 0.000 claims 2
- 125000000999 tert-butyl group Chemical group [H]C([H])([H])C(*)(C([H])([H])[H])C([H])([H])[H] 0.000 claims 2
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 claims 1
- 208000023275 Autoimmune disease Diseases 0.000 claims 1
- 206010005003 Bladder cancer Diseases 0.000 claims 1
- 206010005949 Bone cancer Diseases 0.000 claims 1
- 208000018084 Bone neoplasm Diseases 0.000 claims 1
- 208000003174 Brain Neoplasms Diseases 0.000 claims 1
- 206010006187 Breast cancer Diseases 0.000 claims 1
- 208000026310 Breast neoplasm Diseases 0.000 claims 1
- 125000000882 C2-C6 alkenyl group Chemical group 0.000 claims 1
- 125000003601 C2-C6 alkynyl group Chemical group 0.000 claims 1
- 208000020446 Cardiac disease Diseases 0.000 claims 1
- 206010008342 Cervix carcinoma Diseases 0.000 claims 1
- 206010009944 Colon cancer Diseases 0.000 claims 1
- 208000032612 Glial tumor Diseases 0.000 claims 1
- 206010018338 Glioma Diseases 0.000 claims 1
- 208000008839 Kidney Neoplasms Diseases 0.000 claims 1
- 206010023825 Laryngeal cancer Diseases 0.000 claims 1
- 206010058467 Lung neoplasm malignant Diseases 0.000 claims 1
- 206010025323 Lymphomas Diseases 0.000 claims 1
- 206010029260 Neuroblastoma Diseases 0.000 claims 1
- 206010033128 Ovarian cancer Diseases 0.000 claims 1
- 206010061535 Ovarian neoplasm Diseases 0.000 claims 1
- 206010061902 Pancreatic neoplasm Diseases 0.000 claims 1
- 206010033701 Papillary thyroid cancer Diseases 0.000 claims 1
- 206010060862 Prostate cancer Diseases 0.000 claims 1
- 208000000236 Prostatic Neoplasms Diseases 0.000 claims 1
- 102000001253 Protein Kinase Human genes 0.000 claims 1
- 206010038389 Renal cancer Diseases 0.000 claims 1
- 208000005718 Stomach Neoplasms Diseases 0.000 claims 1
- 208000007097 Urinary Bladder Neoplasms Diseases 0.000 claims 1
- 208000006105 Uterine Cervical Neoplasms Diseases 0.000 claims 1
- 102100025093 Zinc fingers and homeoboxes protein 2 Human genes 0.000 claims 1
- 239000002671 adjuvant Substances 0.000 claims 1
- 125000003545 alkoxy group Chemical group 0.000 claims 1
- 230000000840 anti-viral effect Effects 0.000 claims 1
- 239000002246 antineoplastic agent Substances 0.000 claims 1
- 239000003443 antiviral agent Substances 0.000 claims 1
- 125000002837 carbocyclic group Chemical group 0.000 claims 1
- 201000010881 cervical cancer Diseases 0.000 claims 1
- 238000002512 chemotherapy Methods 0.000 claims 1
- 229940044683 chemotherapy drug Drugs 0.000 claims 1
- 208000029742 colonic neoplasm Diseases 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 206010017758 gastric cancer Diseases 0.000 claims 1
- 208000019622 heart disease Diseases 0.000 claims 1
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 1
- 208000027866 inflammatory disease Diseases 0.000 claims 1
- 239000003112 inhibitor Substances 0.000 claims 1
- 201000010982 kidney cancer Diseases 0.000 claims 1
- 206010023841 laryngeal neoplasm Diseases 0.000 claims 1
- 201000005202 lung cancer Diseases 0.000 claims 1
- 208000020816 lung neoplasm Diseases 0.000 claims 1
- 230000001926 lymphatic effect Effects 0.000 claims 1
- 208000015486 malignant pancreatic neoplasm Diseases 0.000 claims 1
- 230000001404 mediated effect Effects 0.000 claims 1
- 201000001441 melanoma Diseases 0.000 claims 1
- 208000015122 neurodegenerative disease Diseases 0.000 claims 1
- 210000000056 organ Anatomy 0.000 claims 1
- 210000004798 organs belonging to the digestive system Anatomy 0.000 claims 1
- 201000002528 pancreatic cancer Diseases 0.000 claims 1
- 208000008443 pancreatic carcinoma Diseases 0.000 claims 1
- 108060006633 protein kinase Proteins 0.000 claims 1
- 102000009929 raf Kinases Human genes 0.000 claims 1
- 108010077182 raf Kinases Proteins 0.000 claims 1
- 201000011549 stomach cancer Diseases 0.000 claims 1
- 208000030045 thyroid gland papillary carcinoma Diseases 0.000 claims 1
- 201000005112 urinary bladder cancer Diseases 0.000 claims 1
- 239000003981 vehicle Substances 0.000 claims 1
- 230000003612 virological effect Effects 0.000 claims 1
- 0 CC(*)CCC(C)N=C(C)CCC*CC(C)CN Chemical compound CC(*)CCC(C)N=C(C)CCC*CC(C)CN 0.000 description 13
Applications Claiming Priority (7)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US63564404P | 2004-12-13 | 2004-12-13 | |
| US60/635,644 | 2004-12-13 | ||
| US63674004P | 2004-12-16 | 2004-12-16 | |
| US60/636,740 | 2004-12-16 | ||
| US11/301,311 US7767687B2 (en) | 2004-12-13 | 2005-12-12 | Pyrido pyrimidinones, dihydro pyrimido pyrimidinones and pteridinones useful as RAF kinase inhibitors |
| US11/301,311 | 2005-12-12 | ||
| PCT/US2005/044804 WO2006065703A1 (en) | 2004-12-13 | 2005-12-12 | Pyrido pyrimidinones, dihydro pyrimido pyrimidinones and pteridinones useful as raf kinase inhibitors |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2008523099A JP2008523099A (ja) | 2008-07-03 |
| JP2008523099A5 true JP2008523099A5 (enExample) | 2009-02-26 |
| JP5111113B2 JP5111113B2 (ja) | 2012-12-26 |
Family
ID=36097240
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2007545694A Expired - Fee Related JP5111113B2 (ja) | 2004-12-13 | 2005-12-12 | Rafキナーゼ阻害剤として有用なピリドピリミジノン、ジヒドロピリミドピリミジノンおよびプテリジノン |
Country Status (6)
| Country | Link |
|---|---|
| US (2) | US7767687B2 (enExample) |
| EP (1) | EP1828186A1 (enExample) |
| JP (1) | JP5111113B2 (enExample) |
| AU (1) | AU2005316668B2 (enExample) |
| CA (1) | CA2590294A1 (enExample) |
| WO (1) | WO2006065703A1 (enExample) |
Families Citing this family (111)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| PE20100741A1 (es) * | 2005-03-25 | 2010-11-25 | Glaxo Group Ltd | COMPUESTOS DERIVADOS DE 3,4-DIHIDROPIRIMIDO[4,5-d]PIRIMIDIN-2(1H)-ONA COMO INHIBIDORES DE QUINASA p38 |
| EP2270014A1 (en) | 2005-09-22 | 2011-01-05 | Incyte Corporation | Azepine inhibitors of janus kinases |
| NZ594628A (en) | 2005-10-07 | 2013-04-26 | Exelixis Inc | PYRIDOPYRIMIDINONE INHIBITORS OF PI3Ka |
| CN102746298A (zh) | 2005-10-07 | 2012-10-24 | 埃克塞里艾克西斯公司 | PI3Kα的吡啶并嘧啶酮抑制剂 |
| CN101365682A (zh) | 2005-12-08 | 2009-02-11 | 千禧药品公司 | 具有激酶抑制活性的双环化合物 |
| WO2008032162A1 (en) | 2006-09-15 | 2008-03-20 | Pfizer Products Inc. | Pyrido (2, 3-d) pyrimidin0ne compounds and their use as pi3 inhibitors |
| MX2009004077A (es) | 2006-10-19 | 2009-05-05 | Signal Pharm Llc | Compuestos de heteroarilo, composiciones de los mismos, y su uso como inhibidores de proteina cinasas. |
| TW200835497A (en) * | 2007-01-11 | 2008-09-01 | Astrazeneca Ab | Chemical compounds 636 |
| US7799781B2 (en) | 2007-02-01 | 2010-09-21 | Astrazeneca Ab | 5,6,7,8-tetrahydropteridine derivatives as HSP90 inhibitors |
| JP5238172B2 (ja) * | 2007-03-22 | 2013-07-17 | 公益財団法人相模中央化学研究所 | パーフルオロアルキル基を有する含窒素六員環化合物およびその製造方法 |
| NZ582349A (en) * | 2007-06-29 | 2012-06-29 | Sunesis Pharmaceuticals Inc | Heterocyclic compounds useful as raf kinase inhibitors |
| TWI444379B (zh) * | 2007-06-29 | 2014-07-11 | Sunesis Pharmaceuticals Inc | 有用於作為Raf激酶抑制劑之化合物 |
| AU2009289649B2 (en) | 2008-09-03 | 2016-05-05 | Biomarin Pharmaceutical Inc. | Compositions including 6-aminohexanoic acid derivatives as HDAC inhibitors |
| WO2010039740A1 (en) | 2008-09-30 | 2010-04-08 | Exelixis, Inc. | PYRIDOPYRIMIDINONE INHIBITORS OF PI3Kα AND MTOR |
| US8110578B2 (en) | 2008-10-27 | 2012-02-07 | Signal Pharmaceuticals, Llc | Pyrazino[2,3-b]pyrazine mTOR kinase inhibitors for oncology indications and diseases associated with the mTOR/PI3K/Akt pathway |
| JP2012514044A (ja) * | 2008-12-30 | 2012-06-21 | ミレニアム ファーマシューティカルズ, インコーポレイテッド | Rafキナーゼ阻害剤として有用なヘテロアリール化合物 |
| KR101398268B1 (ko) * | 2009-10-23 | 2014-05-23 | 일라이 릴리 앤드 캄파니 | Akt 억제제 |
| JP2013508456A (ja) | 2009-10-26 | 2013-03-07 | シグナル ファーマシューティカルズ, エルエルシー | ヘテロアリール化合物の合成方法および精製方法 |
| EP2992878A1 (en) * | 2010-02-03 | 2016-03-09 | Signal Pharmaceuticals, LLC | Identification of lkb1 mutation as a predictive biomarker for sensitivity to tor kinase inhibitors |
| AR080151A1 (es) | 2010-02-09 | 2012-03-14 | Exelixis Inc | Metodos para tratar cancer usando inhibidores de piridopirimidinona de pi 3k y mtor en combinacion con inhibidores de autofagia |
| WO2012088266A2 (en) | 2010-12-22 | 2012-06-28 | Incyte Corporation | Substituted imidazopyridazines and benzimidazoles as inhibitors of fgfr3 |
| JP6250403B2 (ja) | 2011-02-28 | 2017-12-20 | バイオマリン ファーマシューティカル インク | ヒストン脱アセチル化酵素阻害剤 |
| US8957066B2 (en) | 2011-02-28 | 2015-02-17 | Biomarin Pharmaceutical Inc. | Histone deacetylase inhibitors |
| US10059723B2 (en) | 2011-02-28 | 2018-08-28 | Biomarin Pharmaceutical Inc. | Histone deacetylase inhibitors |
| WO2013049352A2 (en) * | 2011-09-30 | 2013-04-04 | Kineta, Inc. | Anti-viral compounds |
| US9493466B2 (en) | 2011-10-19 | 2016-11-15 | Signal Pharmaceuticals, Llc | Treatment of cancer with TOR kinase inhibitors |
| ES2694413T3 (es) | 2011-12-02 | 2018-12-20 | Signal Pharmaceuticals, Llc | Composiciones farmacéuticas de 7-(6-(2-hidroxipropan-2-il)piridin-3-il)-1-((trans)-4-metoxiciclohexil)-3,4-dihidropirazino [2,3-b]pirazin-2(1H)-ona, una forma sólida de la misma y métodos para su uso |
| HRP20160641T1 (hr) | 2011-12-31 | 2016-09-23 | Beigene, Ltd. | Fuzionirani triciklički spojevi kao inhibitori raf kinaze |
| CA2864905A1 (en) | 2012-02-24 | 2013-08-29 | Signal Pharmaceuticals, Llc | Methods for treating non- small cell lung cancer using tor kinase inhibitor combination therapy |
| HUE042374T2 (hu) | 2012-06-13 | 2019-06-28 | Incyte Holdings Corp | Szubsztituált triciklusos vegyületek mint FGFR inhibitorok |
| US9388185B2 (en) | 2012-08-10 | 2016-07-12 | Incyte Holdings Corporation | Substituted pyrrolo[2,3-b]pyrazines as FGFR inhibitors |
| AU2013203714B2 (en) | 2012-10-18 | 2015-12-03 | Signal Pharmaceuticals, Llc | Inhibition of phosphorylation of PRAS40, GSK3-beta or P70S6K1 as a marker for TOR kinase inhibitory activity |
| US9266892B2 (en) | 2012-12-19 | 2016-02-23 | Incyte Holdings Corporation | Fused pyrazoles as FGFR inhibitors |
| HK1212207A1 (en) | 2013-01-16 | 2016-06-10 | 西格诺药品有限公司 | Substituted pyrrolopyrimidine compounds, compositions thereof, and methods of treatment therewith |
| NZ711376A (en) | 2013-03-15 | 2020-01-31 | Sanofi Sa | Heteroaryl compounds and uses thereof |
| AU2014228746B2 (en) | 2013-03-15 | 2018-08-30 | Celgene Car Llc | Heteroaryl compounds and uses thereof |
| JP6503338B2 (ja) | 2013-03-15 | 2019-04-17 | バイオマリン ファーマシューティカル インコーポレイテッド | Hdac阻害剤 |
| US9321786B2 (en) | 2013-03-15 | 2016-04-26 | Celgene Avilomics Research, Inc. | Heteroaryl compounds and uses thereof |
| CA2909579A1 (en) | 2013-04-17 | 2014-10-23 | Signal Pharmaceuticals, Llc | Combination therapy comprising a tor kinase inhibitor and n-(3-(5-fluoro-2-(4-(2-methoxyethoxy)phenylamino)pyrimidin-4-ylamino)phenyl)acrylamide for treating cancer |
| MX364101B (es) | 2013-04-17 | 2019-04-12 | Signal Pharm Llc | Terapia de combinación que comprende un compuesto de dihidropirazino-pirazina y un antagonista de receptor de andrógenos para tratar cáncer de próstata. |
| HK1221174A1 (zh) | 2013-04-17 | 2017-05-26 | 西格诺药品有限公司 | 用於治疗癌症的包括tor激酶抑制剂和5-取代喹唑啉酮化合物的组合疗法 |
| SG11201508527VA (en) | 2013-04-17 | 2015-11-27 | Signal Pharm Llc | Pharmaceutical formulations, processes, solid forms and methods of use relating to 1-ethyl-7-(2-methyl-6-(1h-1,2,4-triazol-3-yl) pyridin-3-yl) -3,4-dihydropyrazino[2,3-b]pyrazin-2(1h)-one |
| HK1221150A1 (zh) | 2013-04-17 | 2017-05-26 | 西格诺药品有限公司 | 用二氢吡嗪并-吡嗪类对癌症的治疗 |
| WO2014172432A1 (en) | 2013-04-17 | 2014-10-23 | Signal Pharmaceuticals, Llc | Combination therapy comprising a tor kinase inhibitor and a cytidine analog for treating cancer |
| EA030808B1 (ru) | 2013-04-17 | 2018-09-28 | СИГНАЛ ФАРМАСЬЮТИКАЛЗ, ЭлЭлСи | ПРИМЕНЕНИЕ 1-ЭТИЛ-7-(2-МЕТИЛ-6-(1Н-1,2,4-ТРИАЗОЛ-3-ИЛ)ПИРИДИН-3-ИЛ)-3,4-ДИГИДРОПИРАЗИНО[2,3-b]ПИРАЗИН-2(1Н)-ОНА В ЛЕЧЕНИИ МУЛЬТИФОРМНОЙ ГЛИОБЛАСТОМЫ |
| KR102469849B1 (ko) | 2013-04-19 | 2022-11-23 | 인사이트 홀딩스 코포레이션 | Fgfr 저해제로서 이환식 헤테로사이클 |
| AU2014267360B2 (en) | 2013-05-14 | 2018-07-05 | Active Biotech Ab | N-(heteroaryl)-sulfonamide derivatives useful as S100-inhibitors |
| CA3143529A1 (en) | 2013-05-29 | 2014-12-04 | Signal Pharmaceuticals, Llc | Pharmaceutical compositions 0f 7-(6-(2-hydroxypropan-2-yl)pyridin-3-yl)-1-((trans)-4-methoxycyclohexyl)-3,4-dihydropyrazino [2,3-b]pyrazin-2(1h)-one, a solid form thereof and methods of their use |
| MX2015017821A (es) | 2013-07-02 | 2016-04-15 | Syngenta Participations Ag | Heterociclos bi-o triciclicos activos como plaguicidas con sustituyentes que contienen azufre. |
| LT3089971T (lt) | 2014-01-01 | 2020-10-12 | Medivation Technologies Llc | Junginiai ir panaudojimo būdai |
| WO2015160880A1 (en) | 2014-04-16 | 2015-10-22 | Signal Pharmaceuticals, Llc | SOLID FORMS COMPRISING 1-ETHYL-7-(2-METHYL-6-(1H-1,2,4-TRIAZOL-3-YL) PYRIDIN-3-YL)-3,4-DIHYDROPYRAZINO(2,3-b)PYRAZIN-2(1H)-ONE, AND A COFORMER, COMPOSITIONS AND METHODS OF USE THEREOF |
| NZ714742A (en) | 2014-04-16 | 2017-04-28 | Signal Pharm Llc | Solid forms of 1-ethyl-7-(2-methyl-6-(1h-1,2,4-triazol-3-yl)pyridin-3-yl)-3,4-dihydropyrazino[2,3-b]pyrazin-2(1h)-one, compositions thereof and methods of their use |
| US9718824B2 (en) | 2014-04-16 | 2017-08-01 | Signal Pharmaceuticals, Llc | Solid forms comprising 7-(6-(2-hydroxypropan-2-yl)pyridin-3-yl)-1-((trans)-4-methoxycyclohexyl)-3,4-dihydropyrazino[2,3-b]pyrazin-2(1H)-one, and a coformer, compositions and methods of use thereof |
| US9737535B2 (en) | 2014-04-16 | 2017-08-22 | Signal Pharmaceuticals, Llc | Methods for treating cancer using TOR kinase inhibitor combination therapy comprising administering substituted pyrazino[2,3-b]pyrazines |
| NZ629796A (en) | 2014-07-14 | 2015-12-24 | Signal Pharm Llc | Amorphous form of 4-((4-(cyclopentyloxy)-5-(2-methylbenzo[d]oxazol-6-yl)-7h-pyrrolo[2,3-d]pyrimidin-2-yl)amino)-3-methoxy-n-methylbenzamide, compositions thereof and methods of their use |
| KR20170024120A (ko) | 2014-07-14 | 2017-03-06 | 시그날 파마소티칼 엘엘씨 | 치환된 피롤로피리미딘 화합물을 사용한 암의 치료방법, 이의 조성물 |
| JP6689821B2 (ja) | 2014-08-12 | 2020-04-28 | シンジェンタ パーティシペーションズ アーゲー | 硫黄含有置換基を有する殺有害生物的に活性な複素環式誘導体 |
| US10851105B2 (en) | 2014-10-22 | 2020-12-01 | Incyte Corporation | Bicyclic heterocycles as FGFR4 inhibitors |
| BR112017012232B1 (pt) | 2014-12-11 | 2021-08-17 | Syngenta Participations Ag | Derivados tetraciclicos ativos em termos pesticidas com substituintes contendo enxofre |
| UY36548A (es) | 2015-02-05 | 2016-06-01 | Bayer Cropscience Ag | Derivados heterocíclicos condensados bicíclicos sustituidos por 2-(het)arilo como pesticidas |
| UY36547A (es) | 2015-02-05 | 2016-06-01 | Bayer Cropscience Ag | Derivados heterocíclicos condensados bicíclicos sustituidos por 2-(het)arilo como pesticidas |
| AU2016219822B2 (en) | 2015-02-20 | 2020-07-09 | Incyte Holdings Corporation | Bicyclic heterocycles as FGFR inhibitors |
| WO2016134294A1 (en) | 2015-02-20 | 2016-08-25 | Incyte Corporation | Bicyclic heterocycles as fgfr4 inhibitors |
| MA41551A (fr) | 2015-02-20 | 2017-12-26 | Incyte Corp | Hétérocycles bicycliques utilisés en tant qu'inhibiteurs de fgfr4 |
| WO2016162318A1 (de) | 2015-04-08 | 2016-10-13 | Bayer Cropscience Aktiengesellschaft | Kondensierte bicyclische heterocyclen-derivate als schädlingsbekämpfungsmittel und deren zwischenprodukte |
| CN107531682B (zh) | 2015-04-15 | 2021-05-04 | 百济神州有限公司 | B-raf激酶抑制剂的马来酸盐、其结晶形式、制备方法和用途 |
| CA2993312A1 (en) | 2015-07-23 | 2017-01-26 | Takeda Pharmaceutical Company Limited | 1-substituted 1,2,3,4-tetrahydro-1,7-naphthyridin-8-amine derivatives and their use as ep4 receptor antagonists |
| JP6913076B2 (ja) | 2015-08-07 | 2021-08-04 | バイエル・クロップサイエンス・アクチェンゲゼルシャフト | 有害生物防除剤としての2−(ヘタ)アリール−置換縮合ヘテロ環誘導体 |
| JP6916175B2 (ja) | 2015-10-26 | 2021-08-11 | バイエル・クロップサイエンス・アクチェンゲゼルシャフト | 有害生物防除剤としての縮合二環式ヘテロ環誘導体 |
| EP3380470A1 (en) | 2015-11-23 | 2018-10-03 | Syngenta Participations AG | Pesticidally active heterocyclic derivatives with sulphur and cyclopropyl containing substituents |
| WO2017093180A1 (de) | 2015-12-01 | 2017-06-08 | Bayer Cropscience Aktiengesellschaft | Kondensierte bicyclische heterocyclen-derivate als schädlingsbekämpfungsmittel |
| JP6175519B2 (ja) * | 2016-01-04 | 2017-08-09 | ベイジーン リミテッド | Rafキナーゼ阻害剤としての縮合三環式化合物 |
| WO2017144341A1 (de) | 2016-02-23 | 2017-08-31 | Bayer Cropscience Aktiengesellschaft | Kondensierte bicyclische heterocyclen-derivate als schädlingsbekämpfungsmittel |
| WO2017174414A1 (de) | 2016-04-05 | 2017-10-12 | Bayer Cropscience Aktiengesellschaft | Naphthalin-derivate als schädlingsbekämpfungsmittel |
| EP3241830A1 (de) | 2016-05-04 | 2017-11-08 | Bayer CropScience Aktiengesellschaft | Kondensierte bicyclische heterocyclen-derivate als schädlingsbekämpfungsmittel |
| NZ749997A (en) | 2016-07-05 | 2022-11-25 | Beigene Ltd | Combination of a pd-l antagonist and a raf inhibitor for treating cancer |
| ES2877571T3 (es) | 2016-07-19 | 2021-11-17 | Bayer Cropscience Ag | Derivados de heterociclos bicíclicos condensados como pesticidas |
| US10660334B2 (en) | 2016-08-15 | 2020-05-26 | Bayer Cropscience Aktiengesellschaft | Fused bicyclic heterocycle derivatives as pesticides |
| WO2018033448A1 (de) | 2016-08-16 | 2018-02-22 | Bayer Cropscience Aktiengesellschaft | Verfahren zur herstellung von 2-(3,6-dihalopyridin-2-yl)-3h-imidazol[4,5-c]pyridinderivaten und verwandten verbindungen durch umsetzung des 3h-imidazol[4,5-c]pyridinderivats mit einer metallorganischen zink-amin base |
| CN118702706A (zh) | 2016-09-19 | 2024-09-27 | 拜耳作物科学股份公司 | 吡唑并[1,5-a]吡啶衍生物及其作为农药的用途 |
| ES2877814T3 (es) | 2016-10-06 | 2021-11-17 | Bayer Cropscience Ag | Derivados de heterociclos bicíclicos condensados sustituidos con 2-(het)arilo como pesticidas |
| DK3548466T3 (da) | 2016-12-01 | 2022-04-19 | Syngenta Participations Ag | Fremgangsmåde til fremstilling af et mellemprodukt af pesticidaktive heterocykliske derivater med svovlindeholdende substituenter |
| WO2018108671A1 (en) | 2016-12-16 | 2018-06-21 | Basf Se | Pesticidal compounds |
| WO2018138050A1 (de) | 2017-01-26 | 2018-08-02 | Bayer Aktiengesellschaft | Kondensierte bicyclische heterocyclen-derivate als schädlingsbekämpfungsmittel |
| TW201833107A (zh) | 2017-02-06 | 2018-09-16 | 德商拜耳廠股份有限公司 | 作為殺蟲劑之經2-(雜)芳基取代的稠合雜環衍生物 |
| WO2018197257A1 (de) | 2017-04-24 | 2018-11-01 | Bayer Aktiengesellschaft | Kondensierte bicyclische heterocyclen-derivate als schädlingsbekämpfungsmittel |
| AR111960A1 (es) | 2017-05-26 | 2019-09-04 | Incyte Corp | Formas cristalinas de un inhibidor de fgfr y procesos para su preparación |
| MY198676A (en) | 2017-06-22 | 2023-09-15 | Celgene Corp | Treatment of hepatocellular carcinoma characterized by hepatitis b virus infection |
| EP3305786A3 (de) | 2018-01-22 | 2018-07-25 | Bayer CropScience Aktiengesellschaft | Kondensierte bicyclische heterocyclen-derivate als schädlingsbekämpfungsmittel |
| WO2019162174A1 (de) | 2018-02-21 | 2019-08-29 | Bayer Aktiengesellschaft | Kondensierte bicyclische heterocyclen-derivate als schädlingsbekämpfungsmittel |
| MX2020011061A (es) | 2018-04-20 | 2020-11-06 | Bayer Ag | Derivados de heterocicleno como agentes para el control de plagas. |
| EP4309737A3 (en) | 2018-05-04 | 2024-03-27 | Incyte Corporation | Solid forms of an fgfr inhibitor and processes for preparing the same |
| EP3788046B1 (en) | 2018-05-04 | 2025-12-10 | Incyte Corporation | Salts of an fgfr inhibitor |
| EP3636645A1 (de) | 2018-10-11 | 2020-04-15 | Bayer Aktiengesellschaft | Verfahren zur herstellung schwefel-substituierter pyridinderivate |
| CN113710669A (zh) | 2019-02-26 | 2021-11-26 | 拜耳公司 | 作为农药的稠合双环杂环衍生物 |
| KR20210133984A (ko) | 2019-02-26 | 2021-11-08 | 바이엘 악티엔게젤샤프트 | 해충 방제제로서의 축합된 비시클릭 헤테로시클릭 유도체 |
| US11628162B2 (en) | 2019-03-08 | 2023-04-18 | Incyte Corporation | Methods of treating cancer with an FGFR inhibitor |
| AR119140A1 (es) | 2019-06-13 | 2021-11-24 | Pi Industries Ltd | Compuestos heterocíclicos fusionados y su uso como agentes de control de plagas |
| US11591329B2 (en) | 2019-07-09 | 2023-02-28 | Incyte Corporation | Bicyclic heterocycles as FGFR inhibitors |
| US12122767B2 (en) | 2019-10-01 | 2024-10-22 | Incyte Corporation | Bicyclic heterocycles as FGFR inhibitors |
| WO2021076602A1 (en) | 2019-10-14 | 2021-04-22 | Incyte Corporation | Bicyclic heterocycles as fgfr inhibitors |
| WO2021076728A1 (en) | 2019-10-16 | 2021-04-22 | Incyte Corporation | Bicyclic heterocycles as fgfr inhibitors |
| JP7720840B2 (ja) | 2019-12-04 | 2025-08-08 | インサイト・コーポレイション | Fgfr阻害剤としての三環式複素環 |
| KR20220131900A (ko) | 2019-12-04 | 2022-09-29 | 인사이트 코포레이션 | Fgfr 억제제의 유도체 |
| US12012409B2 (en) | 2020-01-15 | 2024-06-18 | Incyte Corporation | Bicyclic heterocycles as FGFR inhibitors |
| CN113912608B (zh) * | 2020-07-10 | 2023-07-14 | 江苏恒瑞医药股份有限公司 | 嘧啶并嘧啶酮类衍生物、其制备方法及其在医药上的应用 |
| CA3215903A1 (en) | 2021-04-12 | 2022-10-20 | Incyte Corporation | Combination therapy comprising an fgfr inhibitor and a nectin-4 targeting agent |
| EP4352059A1 (en) | 2021-06-09 | 2024-04-17 | Incyte Corporation | Tricyclic heterocycles as fgfr inhibitors |
| WO2022261159A1 (en) | 2021-06-09 | 2022-12-15 | Incyte Corporation | Tricyclic heterocycles as fgfr inhibitors |
| WO2025177310A1 (en) | 2024-02-23 | 2025-08-28 | Pi Industries Ltd. | Fused heterocyclic compounds and its uses thereof |
| WO2025177312A1 (en) | 2024-02-23 | 2025-08-28 | Pi Industries Ltd. | Fused heterocyclic compounds and its uses thereof |
Family Cites Families (26)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US5304121A (en) | 1990-12-28 | 1994-04-19 | Boston Scientific Corporation | Drug delivery system making use of a hydrogel polymer coating |
| US5994341A (en) | 1993-07-19 | 1999-11-30 | Angiogenesis Technologies, Inc. | Anti-angiogenic Compositions and methods for the treatment of arthritis |
| US5525711A (en) * | 1994-05-18 | 1996-06-11 | The United States Of America As Represented By The Secretary Of The Department Of Health And Human Services | Pteridine nucleotide analogs as fluorescent DNA probes |
| US6099562A (en) | 1996-06-13 | 2000-08-08 | Schneider (Usa) Inc. | Drug coating with topcoat |
| US6875769B2 (en) | 1996-05-23 | 2005-04-05 | Pfizer Inc. | Substituted6,6-hetero-bicyclicderivatives |
| TW477787B (en) | 1996-08-27 | 2002-03-01 | Pfizer | Pyrido six-membered nitrogen-containing cyclic ring derivatives having corticotropin releasing factor antagonist activity and pharmaceutical composition containing same |
| DE69839338T2 (de) * | 1997-02-05 | 2008-07-10 | Warner-Lambert Company Llc | Pyrido (2,3-d) pyrimidine und 4-amino-pyrimidine als inhibitoren der zellulären proliferation |
| DK1028950T3 (da) | 1997-10-28 | 2003-09-01 | Warner Lambert Co | 7-substituerede quinazolin-2,4-dioner nyttige som antibakterielle midler |
| WO1999051613A1 (en) | 1998-04-03 | 1999-10-14 | Medivir Ab | Prodrugs of phosphorous-containing pharmaceuticals |
| ES2310039T3 (es) | 1998-05-26 | 2008-12-16 | Warner-Lambert Company Llc | Pirimidinas biciclicas y 3,4-dihidropirimidinas biciclicas como inhibidores de la proliferacion celular. |
| US20040044012A1 (en) | 1998-05-26 | 2004-03-04 | Dobrusin Ellen Myra | Bicyclic pyrimidines and bicyclic 3,4-dihydropyrimidines as inhibitors of cellular proliferation |
| WO2001019825A1 (en) * | 1999-09-15 | 2001-03-22 | Warner-Lambert Company | Pteridinones as kinase inhibitors |
| KR20020070520A (ko) | 2000-01-27 | 2002-09-09 | 워너-램버트 캄파니 | 신경퇴행성 질병의 치료를 위한 피리도피리미디논 유도체 |
| GB2359551A (en) * | 2000-02-23 | 2001-08-29 | Astrazeneca Uk Ltd | Pharmaceutically active pyrimidine derivatives |
| AR030053A1 (es) * | 2000-03-02 | 2003-08-13 | Smithkline Beecham Corp | 1h-pirimido [4,5-d] pirimidin-2-onas y sales, composiciones farmaceuticas, uso para la fabricacion de un medicamento y procedimiento para producirlas |
| EP1267876A1 (en) | 2000-03-23 | 2003-01-02 | Merck & Co., Inc. | Thrombin inhibitors |
| DE10050661A1 (de) | 2000-10-13 | 2002-04-18 | Gruenenthal Gmbh | Substituierte 3,4-Dihydro-pyrimido[1,2-a]pyrimidine und 3,4-Dihydro-pyrazino[1,2-a]pyrimidine |
| EP2404603A1 (en) * | 2000-10-23 | 2012-01-11 | Glaxosmithkline LLC | Novel trisubstituted-8H-pyrido[2,3-d]pyrimidin-7-one compounds for the treatment of CSBP/p38 kinase mediated diseases |
| WO2002076954A1 (en) * | 2001-03-23 | 2002-10-03 | Smithkline Beecham Corporation | Compounds useful as kinase inhibitors for the treatment of hyperproliferative diseases |
| PE20030008A1 (es) | 2001-06-19 | 2003-01-22 | Bristol Myers Squibb Co | Inhibidores duales de pde 7 y pde 4 |
| US6511867B2 (en) | 2001-06-30 | 2003-01-28 | Ovonyx, Inc. | Utilizing atomic layer deposition for programmable device |
| EP1474147B1 (en) * | 2001-12-07 | 2010-05-05 | Vertex Pharmaceuticals Incorporated | Pyrimidine-based compounds useful as gsk-3 inhibitors |
| EP1501829B1 (en) * | 2002-05-06 | 2010-11-24 | Vertex Pharmaceuticals Incorporated | Thiadiazoles or oxadiazoles and their use as inhibitors of jak protein kinase |
| WO2004043367A2 (en) | 2002-11-06 | 2004-05-27 | Bristol-Myers Squibb Company | Fused heterocyclic compounds and use thereof |
| KR20060097105A (ko) | 2003-07-22 | 2006-09-13 | 얀센 파마슈티카 엔.브이. | C-fms 키나아제 저해제로서의 퀴놀리논 유도체 |
| CN101711249A (zh) * | 2007-04-11 | 2010-05-19 | 埃克塞里艾克西斯公司 | 作为PI3K-α的抑制剂用于治疗癌症的吡啶并[2,3-D]嘧啶-7-酮化合物 |
-
2005
- 2005-12-12 US US11/301,311 patent/US7767687B2/en not_active Expired - Fee Related
- 2005-12-12 AU AU2005316668A patent/AU2005316668B2/en not_active Ceased
- 2005-12-12 CA CA002590294A patent/CA2590294A1/en not_active Abandoned
- 2005-12-12 JP JP2007545694A patent/JP5111113B2/ja not_active Expired - Fee Related
- 2005-12-12 WO PCT/US2005/044804 patent/WO2006065703A1/en not_active Ceased
- 2005-12-12 EP EP05853671A patent/EP1828186A1/en not_active Withdrawn
-
2010
- 2010-07-26 US US12/843,105 patent/US20110059976A1/en not_active Abandoned
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| JP2008523099A5 (enExample) | ||
| ZA200903300B (en) | Benzazole derivatives, compositions, and methods of use as b-secretase inhibitors | |
| JP2009502801A5 (enExample) | ||
| JP2009526761A5 (enExample) | ||
| JP2009521399A5 (enExample) | ||
| JP2008511633A5 (enExample) | ||
| JP2008506714A5 (enExample) | ||
| Luo et al. | Isoquinolines: Important cores in many marketed and clinical drugs | |
| JP2005507938A5 (enExample) | ||
| JP2008517923A5 (enExample) | ||
| JP2006508965A5 (enExample) | ||
| JP2003519228A5 (enExample) | ||
| JPH0656698A (ja) | 潰瘍胃腸症状の予防もしくは治療用組成物 | |
| JP2005508969A5 (enExample) | ||
| EP1408960B1 (en) | Benz-indole and benzo-quinoline derivatives as prodrugs for tumour treatment | |
| EP1408970B1 (en) | Indolines and tetrahydro-quinolines as prodrugs for tumour treatment | |
| JP2006522023A5 (enExample) | ||
| JP5668092B2 (ja) | 抗腫瘍薬としての5,6,又は7−置換−3−(ヘテロ)アリールイソキノリンアミン誘導体 | |
| RU2007128926A (ru) | Антагонисты 5ht7 рецепторов | |
| JP2006523233A5 (enExample) | ||
| JP2003516994A5 (enExample) | ||
| JP2024525897A (ja) | 変形性関節症の治療におけるnlrp3阻害剤の投与計画 | |
| US8410130B2 (en) | Synthesis of 8H-3A-aza-cyclopenta [A ]indenes and 5,10-dihydropyrrolo[1,2-B]isoquinolines derivatives and their use as antitumor therapeutic agents | |
| JPWO2021147974A5 (enExample) | ||
| TW200533344A (en) | Pharmaceutical compositions for prevention or treatment of overactive bladder associated with neurological disorders |