[EN] FLUORO-METHANESULFONYL-SUBSTITUTED CYCLOALKANOINDOLES AND THEIR USE AS PROSTAGLANDIN D2 ANTAGONISTS [FR] FLUORO-METHANESULFONYL- CYCLOALKANOINDOLES SUBSTITUES ET LEUR UTILISATION EN TANT QU'ANTAGONISTES DE PROSTAGLANDINE D2
原卟啉原氧化酶(PPO,EC 1.3.3.4)已被确定为化学除草剂家族中最重要的作用目标之一,这些除草剂具有一些有趣的特征,例如使用率低,对哺乳动物的毒性低以及对环境的影响小。 。作为开发新的PPO抑制剂的研究工作的继续,通过在C-4和C-5位上的取代基闭环设计并合成了一些重要的PPO抑制性除草剂恶二argyl的苯并噻唑类似物。的生物测定结果表明,该系列8,9,和10具有良好的PPO抑制活性ķ我值范围从0.25至18.63微米。最有趣的是9公升,鉴定了2-((5-(5-叔丁基-2-氧代-1,3,4-恶二唑-2(3 H)-基)-6-氟苯并噻唑-2-基)硫烷基)丙酸乙酯作为其最有前途的候选者,是因为它具有较高的PPO抑制作用(k i = 1.42μM)和在37.5 g ai / ha的浓度下具有广谱的芽后除草活性。
A method of treating pathological blushing is disclosed wherein the patient is administered a DP receptor antagonist. Compositions containing DP antagonists are also included.
揭示了一种治疗病理性面红的方法,其中患者接受DP受体拮抗剂。还包括含有DP拮抗剂的组合物。
Method of treating atherosclerosis, dyslipidemias and related conditions
申请人:——
公开号:US20040229844A1
公开(公告)日:2004-11-18
A method of treating atherosclerosis is disclosed wherein nicotinic acid or another nicotinic acid receptor agonist is administered to the patient in combination with a DP receptor antagonist. The DP receptor antagonist is administered to reduce, prevent or eliminate flushing that may otherwise occur.
The present application relates to indole and indoline derivatives of formula (I), formula (II), formula (III), or formula (IV)
wherein a, R
2
, R
3
, h, k, m, n, L, Q, X, and Z are as defined in the specification. The present application also relates to compositions comprising such compounds, and methods of treating disease conditions using such compounds and compositions.
[EN] SUBSTITUTED TETRAHYDROCARBAZOLE AND CYCLOPENTANOINDOLE DERIVATIVES<br/>[FR] DERIVES DE TETRAHYDROCARBAZOLE ET DE CYCLOPENTANOINDOLE SUBSTITUES
申请人:MERCK FROSST CANADA INC
公开号:WO2005056527A1
公开(公告)日:2005-06-23
The present invention provides substituted tetrahydrocarbazole and cyclopentanoindole derivatives as antagonists of DP receptor, and as such are useful for the treatment of prostaglandin D2 mediated diseases such as rhinitis, asthma and nasal congestion.
The present application relates to indole and indoline derivatives of formula (I)
wherein a, R
1
, R
2
, R
3
, h, i, j, m, n, L, Q, and X are as defined in the specification. The present application also relates to compositions comprising such compounds, and methods of treating disease conditions using such compounds and compositions.