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Spiro-[1,3]-oxazines and spiro-[1,4]-oxazepines as bace1 and/or bace2 inhibitors

一种-cr7ar7b-、-cr2ar2b-的技术，应用在含有效成分的医用配制品、代谢疾病、血液疾病等方向，能够解决低增殖速率等问题

Inactive Publication Date: 2014-02-19
F HOFFMANN LA ROCHE & CO AG
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, BACE2 inhibition combined with Tmem27 siRNA knockdown produces lower proliferation rates

Method used

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  • Spiro-[1,3]-oxazines and spiro-[1,4]-oxazepines as bace1 and/or bace2 inhibitors
  • Spiro-[1,3]-oxazines and spiro-[1,4]-oxazepines as bace1 and/or bace2 inhibitors
  • Spiro-[1,3]-oxazines and spiro-[1,4]-oxazepines as bace1 and/or bace2 inhibitors

Examples

Experimental program
Comparison scheme
Effect test

Embodiment A

[0465] A tablet with the following composition is manufactured in the usual way:

[0466]

[0467] Table 2: Possible tablet composition

[0468] Manufacturing process

[0469] 1. Mix ingredients 1, 2, 3 and 4, and granulate with pure water.

[0470] 2. Dry the granules at 50°C.

[0471] 3. Pass the particles through suitable grinding equipment.

[0472] 4. Add ingredient 5 and mix for three minutes; compress on a suitable press.

Embodiment B-1

[0474] Prepare capsules of the following composition:

[0475]

[0476] Table 3: Possible capsule composition

[0477] Manufacturing process

[0478] 1. Mix ingredients 1, 2 and 3 in a suitable mixer for 30 minutes.

[0479] 2. Add ingredients 4 and 5 and mix for 3 minutes.

[0480] 3. Fill into a suitable capsule.

[0481] The compound of formula I, lactose and corn starch are first mixed in a mixer, and then mixed in a pulverizer. Return the mixture to the mixer; add talc to it and mix thoroughly. The mixture is machine-filled into suitable capsules, such as hard gelatin capsules.

Embodiment B-2

[0483] Prepare soft gelatin capsules with the following composition:

[0484] Ingredients

mg / capsule

Formula I compound

5

Yellow wax

8

Hydrogenated soybean oil

8

Partially hydrogenated vegetable oil

34

Soybean oil

110

Total

165

[0485] Table 4: Composition of possible soft gelatin capsules

[0486] Ingredients

mg / capsule

Gelatin

75

Glycerin 85%

32

Karion83

8 (dry matter)

Titanium dioxide

0.4

Iron Oxide Yellow

1.1

Total

116.5

[0487] Table 5: Possible soft gelatin capsule composition

[0488] Manufacturing process

[0489] The compound of formula I is dissolved in a warm melt of the other ingredients, and the mixture is filled into soft gelatin capsules of appropriate size. Dispose of the filled soft gelatin capsules according to general procedures.

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PUM

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Abstract

The present invention provides spiro-[1,3]-oxazines and spiro-[1,4]-oxazepines of formula I having BACE1 and / or BACE2 inhibitory activity, their manufacture, pharmaceutical compositions containing them and their use as therapeutically active substances. The active compounds of the present invention are useful in the therapeutic and / or prophylactic treatment of e.g. Alzheimer's disease and type 2 diabetes.

Description

Background technique [0001] Alzheimer's disease (AD) is a neurodegenerative disease of the central nervous system and the main cause of progressive dementia in the middle-aged and older population. The clinical symptoms are impaired memory, cognition, temporary and local orientation, judgment and reasoning, and severe mood disorders. There is currently no effective treatment that can prevent the disease or its progression or stably reverse its clinical symptoms. AD has become a major health problem in all societies with high life expectancy, and it has also become a significant economic burden on these social health systems. [0002] AD is characterized by two main pathological features in the central nervous system (CNS): the appearance of amyloid plaques and neurofibrillary tangles (Hardy et al., The amyloid hypothesis of Alzheimer's disease: progress and problems on the road to therapeutics, Science (Science). 2002 Jul19; 297(5580): 353-6, Selkoe, Cell biology of the amyloid ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D498/10A61K31/537A61P25/28
CPCC07D498/10C07D265/18C07D413/04C07D413/12C07D498/20A61P25/28A61P7/12A61P3/10A61K31/537
Inventor 罗伯特·纳尔基齐昂伊曼纽尔·皮纳德沃尔夫冈·沃斯特
Owner F HOFFMANN LA ROCHE & CO AG
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