E. R. Squibb Sons, Inc.

B Richard Vogt

Peter C Wade

Frank L Weisenborn

Thomas P Kissick

Jack Bernstein

Ravi K Varma

Hans Hoehn

David W Cushman

Roland Greenberg

Michael J Antonaccio

Francis A Sowinski

Ligaya M Simpkins

David A Cullison

George C Rovnyak

Ligaya G Magbanua

The degradation of enkephalins in a mammalian host is inhibited by administration of an enkephalinase enzyme inhibitor of the formula ##STR1##

Enkephalinase inhibitors

Radiolabeled steroid derivatives having the formula ##STR1## wherein St is a des-hydroxy steroid moiety of (i) a hydroxy steroid intended for radioimmunoassay or (ii) a hydroxy containing derivative of a steroid intended for radio-immunoassay, said derivative having a strong affinity for the antibodies of the steroid intended for radioimmunoassay; R is hydrogen or alkyl of 1 to 3 carbon atoms; n is 0, 1, 2, 3 or 4 and the asterisk (*) indicates tagging with a radioisotope, are useful as tracers in radioimmunoassays.

Steroid derivatives and their use in radioimmunoassays

Compounds are provided having the structure ##STR1## wherein R.sup.1 is hydrogen, alkyl of 1-3 carbons, phenyl optionally substituted by R.sup.4 ; R.sup.2 is cyano; ##STR2## (wherein Z is a single bond or ##STR3## X is O or S); ##STR4## (wherein R.sup.9 is hydrogen or alkyl, Q is CH or N); ##STR5## wherein R.sup.6 is amino, alkylamino, dialkylamino, haloalkyl or ##STR6## and R.sup.4 and R.sup.5 are the same or different and represent hydrogen, lower alkyl, lower alkoxy, alkanoyloxy, benzyloxy, substituted benzyloxy, hydroxy, halogen (Cl, Br and F), nitro and trifluoromethyl; and R.sup.7, R.sup.8, m and n are as defined hereinafter. The above compounds are useful as anti-allergy agents.

Pyrazolo[1,5-c]quinazoline derivatives and related compounds

Compounds are provided having the structure ##STR1## wherein R.sup.1 is hydrogen or lower alkyl of 1-3 carbons, R.sup.2 is carboxyl, hydroxymethyl, lower alkanoyloxymethyl, or lower alkoxycarbonyl, R.sup.3 is hydrogen, lower alkyl or benzyl, and R.sup.4 and R.sup.5 are the same or different and represent hydrogen, lower alkyl, lower alkoxy, alkanoyloxy, benzyloxy, hydroxy, halogen (Cl, Br and F), nitro, and trifluoromethyl. These compounds are useful as anti-allergics when administered parenterally or by insufflation but have poor activity when administered orally.

Thioxopyrazolo[1,5-c]quinazoline derivatives, anti-allergic compositions

Steroids having as a substituent a group having the formula ##STR1## wherein R is hydrogen or alkyl and n is 0, 1, 2, 3 or 4 are useful as haptens and are also useful when radioiodinated as tracers in radioimmunoassays.

Steroids having a 3-(4-hydroxyphenyl)pentanedioic acid monohydrazide

Compounds having the formula ##STR1## and acid-addition salts thereof, wherein R is hydrogen or alkyl of 1 to 3 carbon atoms and n is 0,1,2,3 or 4 are useful reagents for derivatizing organic compounds to permit the radioiodination of those compounds and their use as tracers in radioimmunoassays, or to permit their use as haptens.

3-(4-Hydroxyphenyl)pentanedioic acid, monohydrazide, derivatives and

Intermediates are provided having the structure ##STR1## wherein X is hydrogen, lower alkyl, lower alkoxy, halogen or trifluoromethyl. These intermediates are useful in preparing pyrazolo[1,5-c]quinazoline anti-allergy compounds.

5-(Optionally substituted 2-aminophenyl)-1H-pyrazole-3-methanol

Radiolabeled steroid derivatives having the formula ##STR1## wherein St is a des-hydroxy steroid moiety of (i) a hydroxy steroid intended for radioimmunoassay or (ii) a hydroxy containing derivative of a steroid intended for radioimmunoassay, said derivative having a strong affinity for the antibodies of the steroid intended for radioimmunoassay; R is hydrogen or alkyl of 1 to 3 carbon atoms; n is 0, 1, 2, 3 or 4 and the asterisk (*) indicates tagging with a radioisotope, are useful as tracers in radioimmunoassays.

Radiolabeled steroid derivatives having the formula ##STR1## wherein St is des-hydroxy steroid moiety of (i) a hydroxy steroid intended for radioimmunoassay or (ii) a hydroxy containing derivative of a steroid intended for radioimmunoassay, said derivative having a strong affinity for the antibodies of the steroid intended for radioimmunoassay; R is hydrogen or alkyl of 1 to 3 carbon atoms; n is 0, 1, 2, 3 or 4 and the asterisk (*) indicates tagging with a radioisotope, are useful as tracers in radioimmunoassays.

Compounds of the following formula ##STR1## are useful as central nervous system depressants, tranquilizers, sedatives, growth promotors, anti-convulsants and muscle relaxants in mammalian species.

Novel 4H-S-triazolo[4,3-A] [1,5]benzodiazepin-5-ones

Radiolabeled vitamin B.sub.12 derivatives having the formula ##STR1## wherein R is hydrogen or alkyl of 1 to 3 carbon atoms; n is 0, 1, 2, 3 or 4; and the asterisk (*) indicates tagging with a radioisotope, are useful as tracers in radioassays.

Vitamin B.sub.12 derivative suitable for radiolabeling

Compounds are provided having the structure ##STR1## wherein R.sup.1 is carboxyl; hydroxymethyl; CO.sub.2 R.sup.3 wherein R.sup.3 is lower alkyl, Li.sup.+, Na.sup.+ or K.sup.+ ; or ##STR2## R.sup.2 is hydrogen, lower alkyl, aryl or trifluoromethyl; and X is hydrogen, lower alkyl, lower alkoxy, halogen (Cl, Br and F), or trifluoromethyl. These compounds are useful as anti-allergics.

Pyrazolo [1,5-C] quinazoline derivatives and their use in treating

Compounds are provided having the structure ##STR1## wherein R.sup.1 and R.sup.2 may be the same or different and R.sup.1 is hydrogen, alkyl of 1-3 carbons, phenyl optionally substituted by R.sup.4 or ##STR2## R.sup.2 is ##STR3## hydrogen, lower alkyl or phenyl optionally substituted by R.sup.4 with the proviso that at least one of R.sup.1 and R.sup.2 is ##STR4## R.sup.3 is hydrogen, lower alkyl, benzyl or phenyl optionally substituted by R.sup.4 ; and R.sup.4 and R.sup.5 are the same or different and represent hydrogen, lower alkyl, lower alkoxy, alkanoyloxy, benzyloxy, benzyloxy having a single mono-lower alkoxy substituent, hydroxy, halogen (Cl, Br and F), nitro, and trifluoromethyl; R.sup.6 is hydrogen, lower alkyl, alkanoyl, aroyl, aralkanoyl, aralkyl or phenyl; and R.sup.7, R.sup.8, m and n are as defined hereinafter.

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Yardley, PA, United States of America

B Richard Vogt