[EN] HETEROCYCLYL PYRAZOLOPYRIMIDINE ANALOGUES AS JAK INHIBITORS<br/>[FR] ANALOGUES D'HÉTÉROCYCLYL PYRAZOLOPYRIMIDINE EN TANT QU'INHIBITEURS DE JAK
申请人:CELLZOME LTD
公开号:WO2011048082A1
公开(公告)日:2011-04-28
The present invention relates to compounds of formula (I) wherein X1 to X5, Y, Z1 to Z3, and R have the meaning as cited in the description and the claims. Said compounds are useful as JAK inhibitors for the treatment or prophylaxis of immunological, inflammatory, autoimmune, allergic disorders, and immunologically-mediated diseases. The invention also relates to pharmaceutical compositions including said compounds, the preparation of such compounds as well as the use as medicaments.
The present invention relates to novel renin inhibitors of general formula (1), novel intermediates involved in their synthesis, their pharmaceutically acceptable salts and pharmaceutical compositions containing them. The present invention also relates to a process of preparing compounds of general formula (1), their tautomeric forms, their pharmaceutically acceptable salts, pharmaceutical compositions containing them, and novel intermediates involved in their synthesis.
Development of novel azabenzofuran TRPA1 antagonists as in vivo tools
作者:Katrina W. Copeland、Alessandro A. Boezio、Eugene Cheung、Josie Lee、Philip Olivieri、Laurie B. Schenkel、Qian Wan、Weiya Wang、Mary C. Wells、Beth Youngblood、Narender R. Gavva、Sonya G. Lehto、Stephanie Geuns-Meyer
DOI:10.1016/j.bmcl.2014.05.069
日期:2014.8
transient receptor potential ankyrin 1 (TRPA1) channel is activated by noxious stimuli including chemical irritants and endogenous inflammatory mediators. Antagonists of this channel are currently being investigated for use as therapeutic agents for treating pain, airway disorders, and itch. A novel azabenzofuran series was developed that demonstrated in vitro inhibition of allyl isothiocyanate (AITC)-induced
瞬时受体电位锚蛋白1(TRPA1)通道被有害刺激物激活,包括化学刺激物和内源性炎症介质。目前正在研究该通道的拮抗剂用作治疗疼痛,气道疾病和瘙痒的治疗剂。开发了一种新型的氮杂苯并呋喃系列,该系列证明了对异硫氰酸烯丙基异氰酸酯(AITC)诱导的45 Ca 2+吸收具有纳摩尔浓度的抗人和大鼠TRPA1的体外抑制作用。从该系列中,化合物10在AITC诱导的大鼠退缩模型中表现出体内靶标覆盖率,同时提供的未结合血浆浓度比TRPA1大鼠IC 50高16倍。
[EN] ALKOXY COMPOUNDS FOR DISEASE TREATMENT<br/>[FR] COMPOSÉS D'ALCOXY POUR LE TRAITEMENT DE MALADIES
申请人:ACUCELA INC
公开号:WO2009045479A1
公开(公告)日:2009-04-09
The present invention relates generally to compositions and methods for treating neurodegenerative diseases and disorders, particularly ophthalmic diseases and disorders. Provided herein are alkoxyl derivative compounds and pharmaceutical compositions comprising these compounds. The subject compositions are useful for treating and preventing ophthalmic diseases and disorders, including age-related macular degeneration (AMD) and Stargardt's Disease.
The present invention relates generally to compositions and methods for treating neurodegenerative diseases and disorders, particularly ophthalmic diseases and disorders. Provided herein are alkoxyl derivative compounds and pharmaceutical compositions comprising these compounds. The subject compositions are useful for treating and preventing ophthalmic diseases and disorders, including age-related macular degeneration (AMD) and Stargardt's Disease.