G.d. Searle & Company

Pharmacia Corporation

C. D. Searle & Co.

Other

Pharmacia Corporation (of Pfizer, Inc.)

John S Baran

Gunnar J Hanson

Mark Andrew Russell

Dave Weissing

Barbara B Chen

Harman S Lowrie

Thomas J Lindberg

Chi-Dean Liang

Donald W Hansen, Jr

Barnett S Pitzele

Robert H Mazur

Alan E Moorman

William H Owens

Tom Lindberg

Doug Steinman

Ivar Laos

Use of propargyl glycine amino propargyl diol compounds for treatment of renal failure

Use of propargyl glycine amino propargyl diol compounds for treatment of congestive heart failure

Use of ethynyl alanine amino diol compounds to inhibit enzymatic conversion of angiotensinogen to angiotensin I

Alkylaminoalkyl-sulfonyl-terminated &bgr;-alanineamide amino-diol compounds for treatment of hypertension

Use of propargyl glycine amino propargyl diol compounds for inhibiting plasma renin activity

Compounds characterized generally as ethynyl alanine amino diol derivatives are useful to treat disorders mediated by plasma renin activity. Compounds of particular interest are renin inhibitors of Formula I

Use of ethynyl alanine amino diol compounds for treatment of renin-mediated disorders

Compounds characterized generally as alkylaminoalkyl-terminated .beta.-alanineamide amino diol derivatives are useful as renin inhibitors for the treatment of hypertension. Compounds of particular interest are those of the formula ##STR1## wherein n is two or three; wherein x is a number selected from zero, one and two; wherein R.sup.2 is selected from hydrido, methyl, ethyl and phenyl; wherein R.sup.3 is selected from hydrido, cyclohexylmethyl, benzyl, fluorobenzyl, chlorobenzyl, napthylmethyl, fluoronaphthylmethyl and chloronaphthylmethyl; wherein R.sup.5 is methyl; wherein R.sup.7 is cyclohexylmethyl; wherein R.sup.8 is selected from n-propyl, isobutyl, cyclopropyl, cyclopropylmethyl, allyl and vinyl; and wherein each of R.sup.9 and R.sup.10 is a group independently selected from methyl, ethyl and isopropyl; or a pharmaceutically-acceptable salt thereof.

Alkylaminoalkyl-sulfonyl-terminated .beta.-alanineamide amino-diol

Compounds characterized generally as ethynyl alanine amino diol derivatives are useful as renin inhibitors for the treatment of cardiovascular disorders. Compounds of particular interest are those of Formula I ##STR1## wherein A is selected from CO and SO.sub.2 wherein X is selected from oxygen atom and methylene; wherein each of R.sub.1 and R.sub.9 is a group independently selected from hydrido, methyl, ethyl, n-propyl, isopropyl, benzyl, .beta.,.beta.,.beta.-trifluoroethyl, t-butyloxycarbonyl and methoxymethylcarbonyl, and wherein the nitrogen atom to which R.sub.1 and R.sub.9 are attached may be combined with oxygen to form an N-oxide; wherein R.sub.2 is selected from hydrido, methyl, ethyl and isopropyl; wherein R.sub.3 is selected from benzyl, cyclohexylmethyl, phenethyl, imidazolemethyl, pyridylmethyl and 2-pyridylethyl; wherein R.sub.5 is propargyl or a propargyl-containing moiety; wherein R.sub.7 is cyclohexylmethyl; wherein each of R.sub.4 and R.sub.6 is independently selected from hydrido and methyl; wherein R.sub.8 is selected from ethyl, n-propyl, isobutyl, cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, cyclopropylmethyl, cyclohexylmethyl, cyclohexylethyl, allyl, vinyl and fluorovinyl; wherein each of R.sub.11 and R.sub.12 is independently selected from hydrido, alkyl and phenyl; wherein m is zero; and wherein n is a number selected from zero through three; or a pharmaceutically-acceptable salt thereof.

Use of ethynyl alanine amino diol compounds for treatment of hypertension

Compounds characterized generally as alkylaminoalkyl-terminated sulfide/sulfonyl-containing cycloalkylalkyl alanine amino-diol derivatives are useful as renin inhibitors for the treatment of hypertension. Compounds of particular interest are those of Formula II: ##STR1## wherein m is is two or three; wherein x is zero or two; wherein R.sup.2 is selected from hydrido, methyl, ethyl and phenyl; wherein R.sup.3 is selected from hydrido, cyclohexylmethyl, benzyl, fluorobenzyl, chlorobenzyl, fluoronaphthylmethyl and chloronaphthylmethyl; wherein R.sup.5 is selected from cycloalkylalkyl groups containing from three to about twelve carbon atoms; wherein R.sup.7 is cyclohexylmethyl; wherein R.sup.8 is selected from n-propyl, isobutyl, cyclopropyl;, cyclopropylmethyl, allyl and vinyl; and wherein each of R.sup.9 and R.sup.10 is a group independently selected from methyl, ethyl and isopropyl; or a pharmaceutically-acceptable salt thereof.

Alkylaminoalkyl-terminated sulfide/sulfonyl-containing

Compounds characterized generally as alkylaminoalkyl-terminated sulfide/sulfonyl-containing cycloalkylalkyl alanine amino-diol derivatives are useful as renin inhibitors for the treatment of hypertension. Compounds of particular interest are those of Formula II: ##STR1## wherein m is two or three; wherein x is zero or two; wherein R.sup.2 is selected from hydrido, methyl, ethyl and phenyl; wherein R.sup.3 is selected from hydrido, cyclohexylmethyl, benzyl, fluorobenzyl, chlorobenzyl, fluoronaphthylmethyl and chloronaphthylmethyl; wherein R.sup.5 is selected from cycloalkylalkyl groups containing from three to about twelve carbon atoms; wherein R.sup.7 is cyclohexylmethyl; wherein R.sup.8 is selected from n-propyl, isobutyl, cyclopropyl, cyclopropylmethyl, allyl and vinyl; and wherein each of R.sup.9 and R.sup.10 is a group independently selected from methyl, ethyl and isopropyl; or a pharmaceutically-acceptable salt thereof.

Propargyl glycine amino use of propargyl diol compounds for treatment of

Use of ethynyl alanine amino diol compounds for treatment of ophthalmic

Non-peptidyl compounds characterized generally as .alpha.-succinamidoacyl aminodiols having an N-phenyl-amino-type group at the N-terminus are useful as renin inhibitors for the treatment of hypertension.

N-phenyl-amino-terminated non-peptidyl .alpha.-succinamidoacyl

Non-peptidyl compounds characterized generally as .alpha.-succinamidoacyl aminodiols having a pyrrolidinyl-type group at the N-terminus are useful as renin inhibitors for the treatment of hypertension.

Pyurrolidinyl-terminated non-peptidyl .alpha.-succinamidoacyl aminodiols

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Winnetka, IL, United States of America

John S Baran