A proline ester represented by the following formula (I): ##STR00001## wherein R.sup.1 represents a hydroxy-lower alkyl group, a lower alkoxy-lower alkyl group, or a lower alkoxy-lower alkoxy-lower alkyl group or a pharmaceutically acceptable salt thereof. The proline ester (I) of the present invention and a pharmaceutically acceptable salt thereof are useful as a prodrug of enalaprilat, which is a medicine useful for preventing or treating circulatory diseases such as hypertension, cardiac diseases (e.g., cardiac hypertrophy, cardiac failure, and myocardial infarct), nephritis, and apoplexy. Thus, a drug containing the ester or a salt thereof is preferably formulated to a percutaneous preparation, particularly a patch, from the viewpoint of medicinal activity and use.

Toaeiyo Ltd.

Proline ester and preparation containing the same for percutaneous administration

Compounds of formula (I) are antagonists of VLA-4 and/or alpha4/beta7, and as such are useful in the inhibition or prevention of cell adhesion and cell-adhesion mediated pathologies. These compounds may be formulated into pharmaceutical compositions and are suitable for use in the treatment of AIDS-related dementia, allergic conjunctivitis, allergic rhinitis, Alzheimer's disease, asthma, atherosclerosis, autologous bone marrow transplantation, certain types of toxic and immune-based nephritis, contact dermal hypersensitivity, inflammatory bowel disease including ulcerative colitis and Crohn's disease, inflammatory lung diseases, inflammatory sequelae of viral infections, meningitis, multiple sclerosis, multiple myeloma, myocarditis, organ transplantation, psoriasis, pulmonary fibrosis, restenosis, rhinitis, rheumatoid arthritis, septic arthritis, stroke, tumor metastasis, uveititis, and type I diabetes.

Merck &amp; Co., Inc.

Substituted N-arylsulfonyl-proline derivatives as potent cell adhesion inhibitors

This invention relates to novel .alpha.-conotoxin-like peptides comprising the following sequence of amino acids: Xaa.sub.1CCSXaa.sub.2Xaa.sub.3Xaa.sub.4CXaa.sub.5Xaa.sub.6Xaa.sub.7Xaa.su- b.8Xaa.sub.9Xaa.sub.10Xaa.sub.11C--NH.sub.2 in which Xaa.sub.1 is G or D; Xaa.sub.3 is proline, hydroxyproline or glutamine; each of Xaa.sub.2 to Xaa.sub.8 and Xaa.sub.11 is independently any amino acid; Xaa.sub.9 is proline, hydroxyproline or glutamine; Xaa.sub.10 is aspartate, glutamate or .gamma.-carboxyglutamate; Xaa.sub.11 is optionally absent; and the C-terminus is optionally amidated, with the proviso that the peptide is not .alpha.-conotoxin Ep1 or .alpha.-conotoxin Im1. The peptides are useful in the treatment or prevention of pain, in recovery from nerve injury, and in the treatment of painful neurological conditions such as stroke.

proline/moždani udar

Proline ester and preparation containing the same for percutaneous administration

Substituted N-arylsulfonyl-proline derivatives as potent cell adhesion inhibitors

.alpha.-conotoxin peptides with analgesic properties

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