专利号:US-8735586-B2 优先权日:2007-06-26 标 题 :Regioselective copper catalyzed synthesis of benzimidazoles and azabenzimidazoles 发明人:ALONSO JORGE; LINDENSCHMIDT ANDREAS; NAZARÉ MARC; URMANN MATTHIAS; HALLAND NIS; RKYEK OMAR 权利人:ALONSO JORGE; LINDENSCHMIDT ANDREAS; NAZARÉ MARC; URMANN MATTHIAS; HALLAND NIS; RKYEK OMAR; SANOFI SA 摘要:The present invention relates to a process for the regioselective synthesis of compounds of the formula I, n nwherein R0; R1; R2; R3; R4; R5; A1; A2; A3; A4, Q and J have the meanings indicated in the claims. The present invention provides a direct copper catalyzed regioselective process to a wide variety of unsymmetrical, multifunctional N-substituted benzimidazoles or azabenzimidazoles of formula I starting from 2-halo-nitroarenes and N-substituted amides.
专利号:EP-2173747-B1 优先权日:2007-06-26 标 题:A regioselective metal catalyzed synthesis of annelated benzimidazoles and azabenzimidazoles 发明人:ALONSO JORGE; LINDENSCHMIDT ANDREAS; NAZARE MARC; R KYEN OMAR; URMANN MATHIAS; HALLAND NIS 权利人:SANOFI SA 摘要:The present invention relates to a process for the regioselective synthesis of compounds of the formula I, wherein R1; R2; R3; R4; J1; J2; J3; J4 and G have the meanings indicated in the claims. The present invention provides a direct metal, e.g. palladium or copper, catalyzed, regioselective process to a wide variety of unsymmetrical, multifunctional N-substituted benzimidazoles or azabenzimidazoles of formula I starting from 2-halo-nitroarenes and N-substituted amides.
专利号:WO-2025128848-A1 优先权日:2023-12-12 标题:Heterocyclic compounds as triggering receptor expressed on myeloid cells 2 agonists and methods of use 发明人:HOUZE JONATHAN B; PANDYA BHAUMIK 权利人:VIGIL NEUROSCIENCE INC 摘要:The present disclosure provides compounds of Formula (I), useful for the activation of Triggering Receptor Expressed on Myeloid Cells 2 ('TREM2'). This disclosure also provides pharmaceutical compositions comprising the compounds, uses of the compounds, and compositions for treatment of, for example, a neurodegenerative disorder. Further, the disclosure provides intermediates useful in the synthesis of compounds of Formula (I).
专利号:WO-2025128873-A1 优先权日:2023-12-12 标题:Heterocyclic pyridinone compounds as triggering receptor expressed on myeloid cells 2 agonists and methods of use 发明人:HOUZE JONATHAN B; PANDYA BHAUMIK 权利人:VIGIL NEUROSCIENCE INC 摘要:The present disclosure provides compounds of Formula (I), useful for the activation of Triggering Receptor Expressed on Myeloid Cells 2 ('TREM2'). This disclosure also provides pharmaceutical compositions comprising the compounds, uses of the compounds, and compositions for treatment of, for example, a neurodegenerative disorder. Further, the disclosure provides intermediates useful in the synthesis of compounds of Formula (I).
专利号:EP-0332033-A2 优先权日:1988-03-11 标 题:N-cyclopropyl anilines and their use in processes for the synthesis of 1-cyclopropyl-quinolone-carboxylic acids and their derivatives 发明人:SCHRIEWER MICHAEL DR; PETERSEN UWE DR; GROHE KLAUS DR; KREBS ANDREAS DR 权利人:BAYER AG 摘要:N-Cyclopropylanilines of the formula (IV) in which R<1>, X<1>, X<2>, X<3>, A, Z and R<2> have the meaning given in the description, which are suitable for the preparation of 4-quinolone- 3-carboxylic acids, and processes for the preparation of quinolone- carboxylic acid derivatives using N-cyclopropylanilines.
专利号:US-10287265-B2 优先权日:2015-03-09 标 题 :Enantiomers of 8-hydroxyquinoline derivatives and the synthesis thereof 发明人:Puskás László; Kanizsai István; PILLOT THIERRY; GYURIS Márió; Szabó András; Takács Ferenc; Hackler László 权利人:AVIDIN CO LTD; SONEAS RES CO LTD; SYNAGING SAS 摘要:Our invention relates to novel enantiomer derivatives of 8-hydroxyquinoline derivatives with general formula (I) and (II) and the synthesis thereof and pharmaceutically acceptable salts and metal complexes thereof, and the medicinal and/or pharmaceutical compositions comprising these compounds. n n n n n n n n n n The essence of the subject matter of the invention relates to the fact that prior art discloses the biological effect and characteristics only of the racemic products, the novel enantiomer derivatives according to the invention appear in our application for the first. n The subject matter of the invention furthermore relates to a novel, stereoselective synthesis for the preparation of the novel enantiomer derivatives according to the invention. The novel medicinal and/or pharmaceutical compositions comprising these enantiomers are suitable for the treatment of the named diseases, and the enanatiomers are used for manufacture of these compositions. These applications for manufacture of the compositions are also the subject matters of the invention. The compounds according to the invention can be used preferably as cytoprotective, neuroprotective, cardioprotective, anxiolytic and antidepressant agent for treatment of neuropsychiatric and neurologic diseases and diseases in connections with transplantations and with ischemia and reperfusion injuries thereof, and inhibition of organ, advantageously skin graft rejection. According to our studies the R-enantiomer has either sole or high biological effect in some cases.
[参考文献]: Mohanad Darawsheh, Et Al. New Mixed Ligand Zinc(Ii) Complexes Based On The Antiepileptic Drug Sodium Valproate And Bioactive Nitrogen-Donor Ligands. Synthesis, Structure And Biological Properties. Eur J Med Chem. 2014 Jul 23:82:152-63.
合成参考文献
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