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Pyrimidinyl amide compounds which inhibit leukocyte adhesion mediated by VLA-4

A compound, alkyl technology, applied in extracellular fluid diseases, drug combinations, organic chemistry, etc., can solve problems such as increased bioavailability and efficacy

Inactive Publication Date: 2008-09-24
ELAN PHARM INC +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Although these compounds have antagonist properties to the binding, increased bioavailability of these compounds would increase their efficacy

Method used

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  • Pyrimidinyl amide compounds which inhibit leukocyte adhesion mediated by VLA-4
  • Pyrimidinyl amide compounds which inhibit leukocyte adhesion mediated by VLA-4
  • Pyrimidinyl amide compounds which inhibit leukocyte adhesion mediated by VLA-4

Examples

Experimental program
Comparison scheme
Effect test

example 1

[0214] Prepare hard gelatin capsules containing the following ingredients:

[0215] Element Quantity (mg / capsule)

[0216] Active ingredient 30.0

[0217] Starch 305.0

[0218] Magnesium Stearate 5.0

[0219] The above ingredients were mixed and filled into hard gelatin capsules in an amount of 340 mg.

example 2

[0221] The tablet formulation is prepared using the following ingredients:

[0222] Element Quantity (mg / tablet)

[0223] Active ingredient 25.0

[0224] Microcrystalline Cellulose 200.0

[0225] Colloidal silicon dioxide 10.0

[0226] Stearic acid 5.0

[0227] The components are blended and compressed to form tablets, each weighing 240 mg.

example 3

[0229] A dry powder inhaler formulation containing the following components is prepared:

[0230] Element weight%

[0231] active ingredient 5

[0232] Lactose 95

[0233] The active ingredient is mixed with lactose and the mixture is added to the dry powder inhaler.

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PUM

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Abstract

Disclosed are compounds which bind VLA-4. Certain of these compounds also inhibit leukocyte adhesion and, in particular, leukocyte adhesion mediated by VLA-4. Such compounds are useful in the treatment of inflammatory diseases in a human or animal subject such as asthma, Alzheimer's disease, atherosclerosis, AIDS dementia, diabetes, inflammatory bowel disease, rheumatoid arthritis, tissue transplantation, tumor metastasis and myocardial ischemia. The compounds can also be administered for the treatment of inflammatory brain diseases such as multiple sclerosis (Formula I).

Description

[0001] Cross References to Related Applications [0002] Pursuant to Title 35, United States Code, Section 119, this application claims priority to co-pending US Provisional Application Serial No. 60 / 722,358, filed September 25, 2005, which is incorporated herein by reference in its entirety. technical field [0003] The present invention relates to compounds which inhibit leukocyte adhesion, especially leukocyte adhesion mediated by α4 integrin, wherein α4 integrin is preferably VLA-4. The invention also relates to pharmaceutical compositions comprising said compounds and methods of using the compounds or pharmaceutical compositions of the invention to treat, for example, inflammation. [0004] references [0005] The following publications are cited in superscript form in this application: [0006] 1 Hemler and Takada, European Patent Application No. 330,506, published 30 August 1989 [0007] 2Elices et al., Cell, 60: 577 584 (1990) [0008] 3 Springer, Nature, 346: 4...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D405/12C07D409/12C07D417/12C07D239/50C07D401/12A61K31/506A61P29/00
CPCC07D403/02C07D239/50C07D401/12C07D405/12C07D409/12C07D417/12A61P1/00A61P1/04A61P1/16A61P11/00A61P11/02A61P11/06A61P13/10A61P13/12A61P17/04A61P17/06A61P19/00A61P19/02A61P21/00A61P25/00A61P25/28A61P27/02A61P29/00A61P35/00A61P35/04A61P37/08A61P43/00A61P7/00A61P7/06A61P9/10A61P3/10A61K31/506
Inventor 克里斯托夫·迈克尔·塞姆科许英姿弗兰克·斯塔潘贝克珍妮弗·莉·史密斯卡桑德拉·伊内兹·罗西特朱里·Y·福田安德烈·W·康拉迪
Owner ELAN PHARM INC
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