Abstract: Compounds of formula (I) are disclosed which are vitronectin receptor antagonists useful in the treatment of osteoporosis.

Abstract: Compounds of formula (I) are disclosed, wherein: A is a fibrinogen antagonist template; W is a linking moiety of the form --(CHR.sup.g).sub.a --U--(CHR.sup.g).sub.b --V--; Q.sup.1, Q.sup.2, Q.sup.3 and Q.sup.4 are independently N or C--R.sup.y, provided that no more than one Q.sup.1, Q.sup.2, Q.sup.3 and Q.sup.4 is N; R' is H or C.sub.1-6 alkyl, C.sub.3-7 cycloalkyl-C.sub.0-6 -alkyl or Ar--C.sub.0-6 alkyl; R.sup.g is H or C.sub.1-6 alkyl, Het-C.sub.0-6 alkyl, C.sub.3-7 cycloalkyl-C.sub.0-6 alkyl or Ar--C.sub.0-6 alkyl; R.sup.k is R.sup.g, --C(O)R.sup.g or --C(O)OR.sup.g R.sup.i is H, C.sub.1-6 alkyl, Het-C.sub.0-6 alkyl, C.sub.3-7 cycloalkyl-C.sub.0-6 alkyl, Ar--C.sub.0-6 alkyl, Het-C.sub.0-6 alkyl--U'--C.sub.1-6 alkyl, C.sub.3-7 cycloalkyl-C.sub.0-6 alkyl--U'--C.sub.1-6 alkyl or Ar--C.sub.0-6 alkyl--U'--C.sub.1-6 alkyl; R.sup.y is H, halo, --OR.sup.g, --SR.sup.g, --CN, --NR.sup.g R.sup.k, --NO.sub.2, --CF.sub.3, CF.sub.3 S(O).sub.r, --CO.sub.2 R.sup.g, --COR.sup.g or --CONR.sup.g.sub.2, or C.sub.

Abstract: Vasopressin antagonists which have a dipeptide tail composed of a neutral and basic amino acid unit demonstrate potent V.sub.1 and V.sub.2 -antagonist activity. Two species of this invention, which are prepared by solid phase peptide synthesis, are [1-(.beta.-mercapto-.beta.,.beta.-cyclopentamethylene propionic acid)-2-(O-ethyl)-D-tyrosine-4-valine-7-tyrosine-8-arginine-9-desglycine]- vasopressin and [1-(.beta.-mercapto-.beta.,.beta.-cyclopentamethylenepropionic acid)-2-(O-ethyl)-D-tyrosine-4-valine-7-arginine-8-tyrosine-9-desglycine]- vasopressin.

Abstract: Vasopressin antagonists which have a tripeptide side chain comprised of three basic amino acids, such as arginine, lysine or ornithine, demonstrate potent V.sub.1 and V.sub.2 -antagonist activity. A species of the invention, which is prepared by conventional peptide sequencing, is [1-(.beta.-mercapto-.beta.,.beta.-cyclopentamethylenepropionic acid)-2-(O-ethyl)-D-tyrosine-4-valine-7-arginine-8-arginine-9-arginine]-va sopression.

Abstract: Vasopressin antagonists which have a dipeptide side chain comprised of two basic amino acids demonstrate potent V.sub.1 and V.sub.2 -antagonist activity. A species of the invention, which is prepared by conventional peptide sequencing, is [1-(.beta.-mercapto-.beta.,.beta.-cyclopentamethylene propionic acid)-2-(O-ethyl)-D-tyrosine-4-valine-7-arginine-8-arginine-9-desglycine]- vasopressin.

Abstract: Peptides having vasopressin antagonist activity are prepared by a peptide synthesizer to insert a N-methylarginine at the 7-position of the structure. An example of this series of compounds is [1-(.beta.-mercapto-.beta.,.beta.-cyclopentamethylenepropionic acid)-2-(O-ethyl-D-tyrosine)-4-valine-7-desproline-8-N-methylarginine-9-de sglycine]-vasopressin.

Abstract: Vasopressin derivatives having V.sub.1 and oxytocin antagonist activity whose structures are characterized by a Mpa unit at position 1 and a des-Pro unit at position 7 are prepared by standard peptide synthetic methods also using an oxidative cyclization of a dimercaptan. Representative species are [1-deaminopenicillamine-2-(O-methyl)-tyrosine-7-desproline-8-arginine-9-de sglycine]vasopressin or [1-.beta.-mercaptopropionic acid-2-D-(O-ethyl)tyrosine-3-isoleucine-4-threonine-7-desproline-8-arginin e-9-desglycine]-vasopressin.

Abstract: Vasopressin derivatives having V.sub.1 and oxytocin antagonist activity whose structures are characterized by a Mpa unit at position 1 and a des-Pro unit at position 7 are prepared by standard peptide synthetic methods also using an oxidative cyclization of a dimercaptan. Representative species are [1-deaminopenicillamine-2-(O-methyl)-tyrosine-7-desproline-8-arginine-9-de sglycine]vasopressin or [1-.beta.-mercaptopropionic acid-2-D-(O-ethyl)tyrosine-3-isoleucine-4-threonine-7-desproline-8-arginin e-9-desglycine]-vasopressin.

Abstract: Certain heptapeptides which have structures characterized by being a six unit cyclic peptide ring with an arginine or lysine tail have vasopressin antagonist activity. An important species of the group is [1-(.beta.-mercapto-.beta.,.beta.-cyclopentamethylenepropionic acid)-2-(O-ethyl-D-tyrosine)-4-valine-7-desproline-8-arginine-9-desglycine ]-vasopressin.

Abstract: Certain octapeptides, which have structures characterized by being a six unit cyclic peptide ring with a dipeptide tail with no proline unit, have vasopressin antagonist activity. An important species of the group is [1-(.beta.-mercapto-.beta.,.beta.-cyclopentamethylenepropionic acid)-2-(O-ethyl-D-tyrosine)-4-valine]-7-desproline-8-arginine-vasopressin .

Abstract: Imidodisulfamide derivatives useful in the treatment of allergic conditions are prepared by reaction of an appropriately substituted tetrahydroisoquinoline and bis-(chlorosulfonyl)imide in the presence of a non-nucleophilic organic base. Pharmaceutical compositions and methods of alleviating the symptoms of an allergic response are also disclosed.

Abstract: Imidodisulfamide derivatives useful in the treatment of allergic conditions are prepared by reaction of an appropriately substituted tetrahydroisoquinoline and bis(chlorosulfonyl)imide in the presence of a tertiary amine. Pharmaceutical compositions and methods of inhibiting the symptoms of an allergic response are also disclosed.

Abstract: Imidodisulfamide derivatives useful in the treatment of allergic conditions are prepared by reaction of an appropriately substituted tetrahydroisoquinoline and bis(chlorosulfonyl)imide in the presence of a tertiary amine.

Abstract: Imidodisulfamide derivatives useful in the treatment of allergic conditions are prepared by reaction of an appropriately substituted primary amine and bis(chlorosulfonyl) imide in the presence of a tertiary amine.