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Compounds for Alzheimer's Disease

A compound, phenyl technology, applied in the field of preventing neurodegenerative diseases, can solve unmet problems

Inactive Publication Date: 2012-02-01
MYRIAD GENETICS
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Therefore, there is a clear unmet need for better and safer medicines

Method used

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  • Compounds for Alzheimer's Disease
  • Compounds for Alzheimer's Disease
  • Compounds for Alzheimer's Disease

Examples

Experimental program
Comparison scheme
Effect test

preparation example Construction

[0729] Preparation of compounds of the present invention

[0730] Representative synthetic schemes and experimental descriptions of compounds of Formulas I-XVI useful in the methods of the invention are given in the Examples below.

[0731] Dosage, Formulation and Route of Administration

[0732] Generally, the active compound of the present invention is administered together with a pharmaceutically acceptable carrier in a therapeutically (or prophylactically) effective amount by any suitable route, such as parenteral, oral or topical administration, according to the above method. The preferred route of administration for use in the present invention is oral administration.

[0733] In general, the toxicity profile and therapeutic efficacy of therapeutic agents can be determined in appropriate models or animal models by standard pharmaceutical procedures. As is known in the art, LD50 represents the dose which is lethal to about 50% of the test population. The ED50 is the...

Embodiment 1

[0746] Embodiment 1: tablet

[0747] components quantity preferred range Compounds of formula I-XVI 400mg +50％--50％ microcrystalline cellulose 392mg +50％--50％

[0748] colloidal silica 4mg +50％--50％ Magnesium stearate 4mg +50％--50％

[0749] Tablets are prepared using known procedures.

Embodiment 2

[0750] Embodiment 2: coated tablet

[0751] components quantity preferred range Compounds of formula I-XVI 400mg +50％--50％ microcrystalline cellulose 392mg +50％--50％ colloidal silica 4mg +50％--50％ Magnesium stearate 4mg +50％--50％ Coating with Lactose Monohydrate, Hydroxypropyl Methyl Cellulose, Titanium Dioxide, Tracetin / Triglyceryl Triacetate, Iron Oxide

[0752] Coated tablets are prepared using known procedures.

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Abstract

The present invention provides novel compounds useful in the treatment of neurodegenerative disorders, including Alzheimer's disease and dementia. These compounds have 2 , -L-C(=O)NH(C 1-3 Alkyl), -L-C(=O)N(C 1-3 alkyl) 2 ,-L-S(=O) 2 (C 1-3 Alkyl), -L-S(=O) 2 NH 2 ,-L-S(=O) 2 N(C 1-3 alkyl) 2 ,-L-S(=O) 2 NH(C 1-3 Alkyl), -L-C(=O)NHOH, -L-C(=O)CH 2 NH 2 , -L-C(=O)CH 2 OH, -L-C(=O)CH 2 SH, -L-C(=O)NHCN, -L-NHC(=O)OR o , -L-C(=O)NHR o , -L-NH(C=O)NHR o , -L-C(=O)N(R o ) 2 , -L-NH(C=O)N(R o ) 2 , -L-sulfo, -L-(2,6-difluorophenol), -L-phosphono and -L-tetrazolyl substituents, wherein L is a linking group.

Description

[0001] Cross References to Related Applications [0002] This application requests U.S. Provisional Application Serial Nos. US 60 / 615,914, filed October 4, 2004; 60 / 616,162, filed October 4, 2004; US 60 / 660,479, filed March 9, 2005; and March 10, 2005 Priority of US 60 / 660,278 filed on , which is hereby incorporated by reference in its entirety. [0003] Technical Field of the Invention [0004] The present invention provides methods for treating neurodegenerative disorders. The invention further provides methods for preventing neurodegenerative disorders. The invention also provides pharmaceutical compositions for use in the methods of the invention. The present invention has applications in the treatment and prevention of neurodegenerative disorders such as Alzheimer's disease, dementia and mild cognitive impairment. Background of the invention [0005] Dementia is a disorder of brain function that seriously affects a person's ability to perform normal daily activities. ...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07D209/04A61K31/404
CPCC07D401/14C07D413/04C07D413/14C07D409/04C07D417/04C07D405/14C07D403/10C07D405/04C07D209/08C07D409/14C07D209/60C07D401/04A61P25/28C07D403/04
Inventor R·斯莱德Y·克里莫娃R·J·霍尔特A·J·云盖W·S·韦纳R·J·沃尔顿J·A·维拉德森M·B·安德森K·扎维茨
Owner MYRIAD GENETICS