IL206854A - Tricyclic compounds as modulators of a – tnf synthesis and 4pde inhibitors - Google Patents
Tricyclic compounds as modulators of a – tnf synthesis and 4pde inhibitorsInfo
- Publication number
- IL206854A IL206854A IL206854A IL20685410A IL206854A IL 206854 A IL206854 A IL 206854A IL 206854 A IL206854 A IL 206854A IL 20685410 A IL20685410 A IL 20685410A IL 206854 A IL206854 A IL 206854A
- Authority
- IL
- Israel
- Prior art keywords
- substituted
- fused
- alkyl
- methoxy
- aryl
- Prior art date
Links
- 150000001875 compounds Chemical class 0.000 title claims description 134
- 230000015572 biosynthetic process Effects 0.000 title description 9
- 238000003786 synthesis reaction Methods 0.000 title description 9
- 229940123932 Phosphodiesterase 4 inhibitor Drugs 0.000 title description 4
- 239000002587 phosphodiesterase IV inhibitor Substances 0.000 title description 4
- 238000000034 method Methods 0.000 claims description 289
- 125000000217 alkyl group Chemical group 0.000 claims description 123
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- -1 alkoxyalkyi Chemical group 0.000 claims description 88
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- 125000000623 heterocyclic group Chemical group 0.000 claims description 75
- 229910052739 hydrogen Inorganic materials 0.000 claims description 69
- 229910052736 halogen Inorganic materials 0.000 claims description 64
- 150000002367 halogens Chemical group 0.000 claims description 64
- 239000001257 hydrogen Chemical group 0.000 claims description 61
- 125000000753 cycloalkyl group Chemical group 0.000 claims description 48
- 229910052757 nitrogen Inorganic materials 0.000 claims description 42
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims description 42
- 125000003342 alkenyl group Chemical group 0.000 claims description 41
- 125000003545 alkoxy group Chemical group 0.000 claims description 39
- 125000000304 alkynyl group Chemical group 0.000 claims description 39
- 150000003839 salts Chemical class 0.000 claims description 36
- 239000008194 pharmaceutical composition Substances 0.000 claims description 32
- 125000001188 haloalkyl group Chemical group 0.000 claims description 30
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims description 28
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- 238000011282 treatment Methods 0.000 claims description 25
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- 125000004093 cyano group Chemical group *C#N 0.000 claims description 23
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 claims description 23
- 230000000694 effects Effects 0.000 claims description 20
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims description 20
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical group [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims description 18
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims description 16
- 125000004350 aryl cycloalkyl group Chemical group 0.000 claims description 15
- 125000000852 azido group Chemical group *N=[N+]=[N-] 0.000 claims description 15
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- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims description 8
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- 239000003112 inhibitor Substances 0.000 description 21
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Applications Claiming Priority (2)
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| US2361708P | 2008-01-25 | 2008-01-25 | |
| PCT/US2009/031819 WO2009094528A1 (en) | 2008-01-25 | 2009-01-23 | TRICYCLIC COMPOUNDS AS MODULATORS OF TNF-α SYNTHESIS AND AS PDE4 INHIBITORS |
Publications (2)
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| IL206854A0 IL206854A0 (en) | 2010-12-30 |
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| US7964608B2 (en) * | 2008-01-25 | 2011-06-21 | High Point Pharmaceuticals, Llc | Tricyclic compounds as modulators of TNF-α synthesis |
| US8754114B2 (en) | 2010-12-22 | 2014-06-17 | Incyte Corporation | Substituted imidazopyridazines and benzimidazoles as inhibitors of FGFR3 |
| AR090100A1 (es) * | 2012-02-21 | 2014-10-22 | Celgene Corp | Procesos para la preparacion de la (s)-1-(3-etoxi-4-metoxifenil)-2-metanosulfoniletilamina |
| EP3495367B1 (en) | 2012-06-13 | 2020-09-30 | Incyte Holdings Corporation | Substituted tricyclic compounds as fgfr inhibitors |
| WO2014026125A1 (en) | 2012-08-10 | 2014-02-13 | Incyte Corporation | Pyrazine derivatives as fgfr inhibitors |
| US9266892B2 (en) | 2012-12-19 | 2016-02-23 | Incyte Holdings Corporation | Fused pyrazoles as FGFR inhibitors |
| CN108250142B (zh) | 2013-02-01 | 2021-01-26 | 维尔斯达医疗公司 | 具有抗炎、抗真菌、抗寄生物和抗癌活性的胺化合物 |
| DK2986610T5 (en) | 2013-04-19 | 2018-12-10 | Incyte Holdings Corp | BICYCLIC HETEROCYCLES AS FGFR INHIBITORS |
| US10851105B2 (en) | 2014-10-22 | 2020-12-01 | Incyte Corporation | Bicyclic heterocycles as FGFR4 inhibitors |
| CR20170390A (es) | 2015-02-20 | 2017-10-23 | Incyte Holdings Corp | Heterociclos biciclicos como inhibidores de fgfr |
| 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 |
| UA125334C2 (uk) * | 2015-06-17 | 2022-02-23 | Пфайзер Інк. | Трициклічні сполуки та їх застосування як інгібіторів фосфодіестерази |
| WO2017089347A1 (en) | 2015-11-25 | 2017-06-01 | Inserm (Institut National De La Sante Et De La Recherche Medicale) | Methods and pharmaceutical compositions for the treatment of braf inhibitor resistant melanomas |
| EP4467565A3 (en) | 2016-12-21 | 2025-03-12 | Amgen Inc. | Anti-tnf alpha antibody formulations |
| AR111960A1 (es) | 2017-05-26 | 2019-09-04 | Incyte Corp | Formas cristalinas de un inhibidor de fgfr y procesos para su preparación |
| US11466004B2 (en) | 2018-05-04 | 2022-10-11 | Incyte Corporation | Solid forms of an FGFR inhibitor and processes for preparing the same |
| CN112566912A (zh) | 2018-05-04 | 2021-03-26 | 因赛特公司 | Fgfr抑制剂的盐 |
| CN109705037A (zh) * | 2019-01-24 | 2019-05-03 | 广西师范大学 | 4-氨基喹啉-3-甲酸酯衍生物及其制备方法和应用 |
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| BR112022010664A2 (pt) | 2019-12-04 | 2022-08-16 | Incyte Corp | Derivados de um inibidor de fgfr |
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| JPH0741479A (ja) * | 1993-07-28 | 1995-02-10 | Taisho Pharmaceut Co Ltd | ７−アザプテリジン類およびその製造方法 |
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| US6930101B1 (en) * | 1999-05-17 | 2005-08-16 | The Regents Of The University Of California | Thiazolopyrimidines useful as TNFα inhibitors |
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