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)

Start Date01 Mar 2015

Sponsor / Collaborator

Boehringer Ingelheim GmbH

NCT02254161 / TerminatedPhase 1

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.

Start Date01 Nov 2014

Sponsor / Collaborator

Boehringer Ingelheim GmbH

NCT02106247 / CompletedPhase 1

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.

Start Date01 Apr 2014

Sponsor / Collaborator

Boehringer Ingelheim GmbH

100 Clinical Results associated with BI-1181181

100 Translational Medicine associated with BI-1181181

100 Patents (Medical) associated with BI-1181181

Literatures (Medical) associated with BI-1181181

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

Author: 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 Deals associated with BI-1181181

R&D Status

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Indication	Highest Phase	Country/Location	Organization	Date
Alzheimer Disease	Phase 1	DE	Boehringer Ingelheim GmbH	-
Alzheimer Disease	Phase 1	BE	Boehringer Ingelheim GmbH	-
Alzheimer Disease	Phase 1	-	Vitae Pharmaceuticals LLC	-
Alzheimer Disease	Phase 1	-	C.H. Boehringer Sohn AG & Co. KG	-

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Study	Phase	Population	Analyzed Enrollment	Group	Results	Evaluation	Publication Date


AAIC2015	Not Applicable	-	36	BI 1181181 50 mg	artnowbnpx(xcqryhsqyq) = The majority of AEs were of mild and moderate intensity. Severe AEs, all procedural headaches, occurred in 6 subjects (16.7%) arhhhfwzza (opcfcqpiky ) View more	-	01 Jul 2015
				BI 1181181 100 mg

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