Abstract: The present invention relates to compounds of the formula ##STR1## and pharmaceutical compositions containing a therapeutically effective amount of the compounds in combination with a pharmaceutically acceptable carrier and a method for treating diseases mediated by platelet activating factor.
Type:
Grant
Filed:
October 2, 1996
Date of Patent:
July 29, 1997
Assignee:
C.D. Searle & Co.
Inventors:
Ish Kumar Khanna, Michael Allan Stealey, Richard Mathias Weier
Abstract: A class of N-arylheteroarylalkyl 1-heteroaryl-imidazol-2-one compounds is described for use in treatment of glaucoma disorder. Compounds of particular interest are angiotensin II antagonists of the formula ##STR1## wherein A is selected from ##STR2## wherein R.sup.1 is selected from hydrido and alkyl; wherein each of R.sup.2, R.sup.3 and R.sup.4 is independently selected from hydrido, alkyl, alkoxy, halo, hydroxy, carboxyl, alkoxycarbonyl, formyl and acetyl; wherein R.sup.5 is hydrido; wherein R.sup.6 is alkyl; wherein R.sup.7 is an acidic group selected from COOH and ##STR3## or a stereoisomer or a tautomer thereof or a pharmaceutically-acceptable salt thereof.
Abstract: Non-peptidyl compounds characterized generally as .alpha.-succinamidoacyl aminodiols having a 1,3-thiomorpholino-type group or a 1,4-thiomorpholino-type group at the N-terminus are useful as renin inhibitors for the treatment of hypertension.
Abstract: Compounds characterized generally as being propargyl-terminated aryl/alkylsulfonyl-terminated amino diol derivatives having a cycloalkylalkyl group at the P2 substitution site are useful as renin inhibitors for the treatment of hypertension. Compounds of particular interest are those of the formula ##STR1## wherein R.sup.1 is selected from isopropyl, isobutyl, sec-butyl, tert-butyl, phenyl, fluorophenyl, chlorophenyl, benzyl, fluorobenzyl, chlorobenzyl, naphthyl, fluoronaphthyl, chloronaphthyl, fluoronaphthylmethyl and chloronaphthylmethyl; 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; and wherein R.sup.8 is propargyl or a propargyl-containing moiety.
Type:
Grant
Filed:
July 20, 1992
Date of Patent:
December 7, 1993
Assignee:
C. D. Searle & Co.
Inventors:
Gunnar J. Hanson, Barbara B. Chen, John S. Baran
Abstract: Compositions containing certain indole-2-carboxylate compounds and derivatives are described as being therapeutically effective in treatment of CNS disorders resulting from neurotoxic damage or neurodegenerative diseases, particularly those CNS disorders resulting from ischemic events. Preferred compounds are of the formula ##STR1## wherein each of R.sup.5 and R.sup.6 is independently selected from hydrido, bromo, chloro and fluoro, and wherein each of R.sup.10 and R.sup.12 is independently selected from hydrido and lower alkyl, and pharmaceutically-acceptable salts thereof.
Type:
Grant
Filed:
March 1, 1990
Date of Patent:
August 11, 1992
Assignee:
C.D. Searle & Co.
Inventors:
Nancy M. Gray, Brian K. Cheng, William F. Hood, Michael S. Dappen, Alex A. Cordi
Abstract: This invention related to leukotriene B.sub.4 antagonists having the structure ##STR1## and the pharmaceutically acceptable addition salts thereof; wherein R.sup.1 is lower alkyl having 1-10 carbon atoms; or lower alkenyl or alkynyl having 2-10 carbon atoms; or lower alkadienyl having 3-10 carbon atoms; or lower alkadienyl or alkenynyl having 4-10 carbon atoms;wherein R.sup.2 and R.sup.3 are the same or different and represent hydrogen or lower alkyl having 1-6 carbon atoms;wherein X is CH.dbd.CH, S, or O;wherein Y is CH.dbd.CH or C.tbd.C;wherein Z is OR.sup.4 or NR.sup.5 R.sup.6, and wherein R.sup.4 represents H, lower alkyl having 1-6 carbon atoms, or a pharmaceutically acceptable cation, and wherein R.sup.5 and R.sup.6 act independently and represent H or lower alkyl having 1-6 carbon atoms, or R.sup.5 and R.sup.
Type:
Grant
Filed:
June 3, 1988
Date of Patent:
January 23, 1990
Assignee:
C. D. Searle & Co.
Inventors:
Stevan W. Djuric, Richard A. Haack, Julie M. Miyashiro