To assess the influence of different dose strengths of BI 1181181 on single dose kinetics of midazolam (CYP3A4 probe drug), warfarin (CYP2C9 probe drug), omeprazole (CYP2C19 probe drug) and digoxin (P-gp probe drug)

开始日期2015-03-01

申办/合作机构

Boehringer Ingelheim GmbH

NCT02254161 / Terminated临床1期

Safety, Tolerability, Pharmacokinetics, and Pharmacodynamics of Multiple Rising Doses of BI 1181181 Given Orally q.d. for 10 Days in Young Healthy Male and Elderly Healthy Male/Female Volunteers (Randomized, Double-blind, Placebo Controlled Within Dose Groups Phase I Study)

The primary objective of the current study is to investigate the safety and tolerability of BI 1181181 in healthy young male and elderly male and female volunteers following oral administration of repeated rising doses of BI 1181181, given once daily over 10 days. Secondary objectives are the exploration of the pharmacokinetics (PK) and pharmacodynamics (PD) of BI 1181181.

开始日期2014-11-01

申办/合作机构

Boehringer Ingelheim GmbH

NCT02106247 / Completed临床1期

Safety, Tolerability, Pharmacokinetics and Pharmacodynamics of Single Oral Doses of BI 1181181 in Young Healthy Male Volunteers (Randomised, Double-blind, Placebo-controlled Within Dose Groups Phase I Trial)

To assess the reduction of ß-amyloid levels in cerebrospinal fluid and plasma and to evaluate pharmacokinetics, safety and tolerability following single oral doses of BI 1181181.

开始日期2014-04-01

申办/合作机构

Boehringer Ingelheim GmbH

100 项与 BI-1181181 相关的临床结果

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100 项与 BI-1181181 相关的转化医学

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100 项与 BI-1181181 相关的专利（医药）

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项与 BI-1181181 相关的文献（医药）

Journal of labelled compounds & radiopharmaceuticals

Synthesis of beta-site amyloid precursor protein-cleaving enzyme 1 inhibitors BI 1147560 and BI 1181181 labeled with carbon-14 and deuterium.

Article

作者: Latli, Bachir ; Hrapchak, Matt J. ; Song, Jinhua J. ; Lee, Heewon ; Reeves, Jonathan T.

The generation of amyloid beta peptides that aggregate in the brain is believed to play a major role in Alzheimer's disease. In theory, the inhibition of beta-site amyloid precursor protein-cleaving enzyme 1 (BACE1), which catalyzes the initial rate-limiting step in amyloid beta production, may slow or stop Alzheimer's disease. Herein, we report the preparation of two potent BACE1 inhibitors, BI 1147560 (1) and BI 1181181 (2), labeled with carbon-14 and with deuterium. The use of advanced key chiral intermediates like 3 and 5 shortened the carbon-14 syntheses of these two compounds to five and six steps, respectively, and helped in preparing them with very high chemical purity and enantiomeric excess without deviating from the process chemistry route. For the deuterium synthesis, oxetan-3-ylmethanamine [² H₆ ]-7 and 2-fluoro-2-methylpropan-1-amine [² H₆ ]-9 were prepared then used with the chiral intermediate 5 to furnish deuterium labeled 1 and 2, respectively.

100 项与 BI-1181181 相关的药物交易

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研发状态

10 条进展最快的记录,

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适应症	最高研发状态	国家/地区	公司	日期
阿尔茨海默症	临床1期	德国	Boehringer Ingelheim GmbH	-
阿尔茨海默症	临床1期	比利时	Boehringer Ingelheim GmbH	-
阿尔茨海默症	临床1期	-	Vitae Pharmaceuticals LLC	-
阿尔茨海默症	临床1期	-	C.H. Boehringer Sohn AG & Co. KG	-

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临床结果

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研究	分期	人群特征	评价人数	分组	结果	评价	发布日期


AAIC2015	N/A	-	36	BI 1181181 50 mg	顧觸齋窪廠膚齋憲獵鏇(窪齋願選遞衊積醖遞選) = The majority of AEs were of mild and moderate intensity. Severe AEs, all procedural headaches, occurred in 6 subjects (16.7%) 範淵築窪遞製壓廠襯醖 (齋繭衊襯鬱鹽繭範鹽繭 ) 更多	-	2015-07-01
				BI 1181181 100 mg