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Heterocyclic compounds which inhibit leukocyte adhesion mediated by alpha4 integrins

A compound, azetidinyl technology, used in the field of compounds for white blood cell adhesion

Inactive Publication Date: 2007-05-09
ELAN PHARM INC
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Although these compounds are antagonistic to such binding, increased bioavailability of these compounds will enhance their potency

Method used

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  • Heterocyclic compounds which inhibit leukocyte adhesion mediated by alpha4 integrins
  • Heterocyclic compounds which inhibit leukocyte adhesion mediated by alpha4 integrins
  • Heterocyclic compounds which inhibit leukocyte adhesion mediated by alpha4 integrins

Examples

Experimental program
Comparison scheme
Effect test

preparation example

[0139] For the preparation of solid compositions such as tablets, the principal active ingredient can be mixed with a pharmaceutical excipient to form a solid preformulated composition comprising a homogeneous mixture of a compound of the invention. When these pre-formulated compositions are referred to as homogeneous, it is meant that the active ingredient is diffused uniformly throughout the composition such that the composition can be easily subdivided into equivalent unit dosage forms such as tablets, pills and capsules . This solid pre-formulation is then subdivided into unit dosage forms of the type described above containing, for example, from about 0.1 to about 500 mg of the active ingredient of the invention.

[0140] The tablets or pills of the present invention may be coated or otherwise formulated to provide a dosage form which has the advantage of prolonged action. For example, the tablet or pill may comprise an inner dosage component and an outer dosage componen...

example 1

[0145] Prepare hard gelatin capsules containing the following ingredients:

[0146] quantity

[0147] Composition (mg / capsule)

[0148] Active ingredient 30.0

[0149] Starch 305.0

[0150] Magnesium Stearate 5.0

[0151] The above ingredients were mixed and filled into hard gelatin capsules in an amount of 340 mg.

example 2

[0153] A tablet formulation is prepared with the following ingredients:

[0154] quantity

[0155] Composition (mg / tablet)

[0156] Active ingredient 25.0

[0157] Microcrystalline Cellulose 200.0

[0158] Colloidal silica 10.0

[0159] Stearic acid 5.0

[0160] The ingredients are mixed and compressed into tablets, each weighing 240 mg.

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PUM

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Abstract

Disclosed are compounds which bind alpha4 integrins, preferably VLA-4. Certain of these compounds also inhibit leukocyte adhesion and, in particular, leukocyte adhesion mediated by alpha4 integrins, preferably VLA-4. Such compounds are useful in the treatment of inflammatory diseases in a mammalian patient, e.g., human, 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.

Description

technical field [0001] The present invention relates to the ability to inhibit leukocyte adhesion and especially by alpha 4 Integrin-mediated leukocyte adhesion compound in which α 4 The integrin is preferably VLA-4. [0002] reference technology [0003] In this patent case, the following publications, patents and patent applications are cited in the form of the above symbols: [0004] 1 Hemler and Takada, European Patent Application No. 330,506, published August 30,1989. [0005] 2 Alices, et al., Cell, 60 : 577-584 (1990) [0006] 3 Springer, Nature, 346 : 425-434 (1990) [0007] 4 Osborne, Cell. 62 : 3-6 (1990) [0008] 5 Vedder, et al., Surgery, 106 : 509 (1989) [0009] 6 Pretolani, et al., J. Exp. Med., 180 : 795 (1994) [0010] 7 Abraham, et al., J. Clin. Invest, 93 : 776 (1994) [0011] 8 Mulligan, et al., J. Immunology, 150 : 2407 (1993) [0012] 9 Cybulsky, et al., Science, 251 : 788 (1991) [0013] 10 Li, et al., Arteriosckr. Thromb., ...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07D401/10A61P19/02A61P29/00C07D239/69A61K31/505A61K31/506A61P43/00C07D239/50C07D401/12C07D403/12
CPCC07D401/12C07D403/12C07D239/50A61P1/04A61P11/06A61P19/02A61P25/00A61P25/28A61P29/00A61P35/04A61P37/06A61P43/00A61P9/10A61P3/10
Inventor 安德烈·W·康拉迪克里斯托夫·M·塞姆科许英姿弗兰克·斯塔潘贝克布赖恩·P·斯图皮珍妮弗·史密斯尤金·D·托尔塞特迈克尔·A·普莱斯
Owner ELAN PHARM INC
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