Abstract: Phenolic esters of the general formula I ##STR1## are useful for the prevention, management or alleviation of elastase mediated diseases or conditions.
Abstract: The invention relates to compounds of the formula: ##STR1## which are useful as leukotriene D.sub.4 (LTD.sub.4) inhibitors and therefore useful in the treatment of allergies and inflammatory conditions.
Type:
Grant
Filed:
August 12, 1985
Date of Patent:
May 12, 1987
Assignee:
G. D. Searle & Co.
Inventors:
Masateru Miyano, Robert L. Shone, Daniel D. Sohn
Abstract: Compositions of matter are disclosed of compounds of the formula ##STR1## and the pharmaceutically acceptable acid addition salts thereof wherein X represents a halo, lower alkyl, hydrogen, trifluoromethyl, phenyl, or lower alkoxy substituent; Y represents --CN, --CONH.sub.2, --CON(R.sub.1).sub.2 or --CO.sub.2 R.sub.1 where R.sub.1 is a lower alkyl; m is the integer 1 or 2 and n is an integer from 1 to 3 inclusive; R.sub.2 represents lower alkyl; R.sub.3 represents lower alkyl or acetyl, aroyl, phenacetyl or trifluoracetyl; A, B, and D are carbonyl or methylene such that when one of A, B, or D is carbonyl, the others are methylene and R.sub.3 is lower alkyl, whereas when R.sub.3 is acetyl, aroyl, phenacetyl or trifluoroacetyl, A, B, and D are methylene. These compounds have utility as antiarrhythmic agents.
Type:
Grant
Filed:
July 9, 1984
Date of Patent:
January 27, 1987
Assignee:
G. D. Searle & Co.
Inventors:
Bipinchandra N. Desai, Robert J. Chorvat, Kurt J. Rorig
Abstract: Compounds of formula I ##STR1## are described which are useful to inhibit the formation of serum cholesterol by virtue of their ability to inhibit .beta.-hydroxy-.beta.-methylglutaryl-CoA(HMG CoA), the rate-controlling substance in the synthesis of serum cholesterol.
Type:
Grant
Filed:
March 11, 1985
Date of Patent:
November 11, 1986
Assignee:
G. D. Searle & Co.
Inventors:
John S. Baran, Thomas J. Lindberg, Harman S. Lowrie
Abstract: The present invention provides novel compounds of Formula I ##STR1## which are pharmacologically selectively useful as anti-thrombotic agents with minimal blood pressure lowering activity.
Abstract: Kojic acid ether-ester derivatives of formula I ##STR1## are useful pharmacological agents for the prevention, management or alleviation of elastase mediated diseases or conditions.
Abstract: This invention relates to methods of preventing or reducing the degradation of elastin and other proteins and thereby preventing or retarding the disease states caused by said degradation by administering compounds of the formula: ##STR1## or their pharmacologically acceptable salts.
Abstract: This invention relates to novel allenic prostanoic acid derivatives having the following formula ##STR1## wherein R is hydrogen; or straight or branched chain alkyl of 1 to 6 carbon atoms, inclusivewherein R.sub.1 is hydrogen; or straight or branched chain alkyl of 1 to 6 carbon atoms, inclusive; or vinyl (--CH.dbd.CH.sub.2)wherein R.sub.2 is straight or branched chain alkyl of 1 to 6 carbon atoms; or cycloalkyl group containing 3 to 6 carbon atoms; or phenyl; or phenoxywherein R.sub.3 is hydrogen; or straight chain alkyl of 1 to 3 carbon atomswherein m is an integer of from 1 to 4, inclusive,wherein n is an integer of from 1 to 3, inclusive with the proviso that the sum of m and n does not exceed 5,wherein y is an integer of from 1 to 3.These compounds are useful by reason of their gastric antisecretory and cytoprotective activity.
Abstract: This invention relates to hexahydroindolizinones, which are useful as inhibitors of cardiac arrhythmias and of platelet aggregation and are therefore useful in the treatment of irregular heartbeat and in the prevention of thrombus formation.
Type:
Grant
Filed:
September 17, 1984
Date of Patent:
January 28, 1986
Assignee:
G. D. Searle & Co.
Inventors:
Robert J. Chorvat, Kathleen A. Prodan, John A. Schulz
Abstract: The invention relates to substituted dihydrobenzopyrans carboxylates of the formula: ##STR1## wherein A is a methylene chain having 1-10 carbon atoms, inclusive, optionally substituted by hydroxy;wherein V is:(a) hydrogen;(b) hydroxy;(c) .dbd.O; or(d) R.sub.6 CH.sub.2 O--;wherein R.sub.1 is:(a) --COCH.sub.3 ;(b) --CHOHCH.sub.3 ;(c) --C.sub.2 H.sub.5 ;(d) -hydrogen; or(e) --COOC.sub.2 H.sub.5wherein R.sub.2 is:(a) -hydrogen;(b) -hydroxy; or(c) R.sub.12 CH.sub.2 CO.sub.2 --;wherein R.sub.3, R.sub.4, R.sub.6, R.sub.7, R.sub.8, R.sub.9, R.sub.10, R.sub.11 and R.sub.12 each of which may be the same or different, are:(a) hydrogen;(b) lower-alkyl having 1-6 carbon atoms inclusive; or(c) allyl;wherein R.sub.5 is:(a) hydrogen; or(b) R.sub.7 CH.sub.2 C(O)--;wherein R.sub.13 is hydrogen, hydroxy, alkoxy of 1 to 6 carbon atoms inclusive, or --OM wherein M is an alkali metal, alkyl of 1 to 6 carbon atoms, inclusive, or NR.sub.8.sup..sym. R.sub.9 R.sub.10 R.sub.11, or HNR.sub.8.sup..sym. R.sub.9 R.sub.
Abstract: This invention relates to substituted chromanon-2-yl alkanols and derivatives thereof, which are useful as leukotriene D.sub.4 (LTD.sub.4) inhibitors and therefore useful in the treatment of allergies, inflammatory conditions, and coronary vasoconstriction.
Type:
Grant
Filed:
May 29, 1984
Date of Patent:
October 8, 1985
Assignee:
G. D. Searle & Co.
Inventors:
Masateru Miyano, Clara I. Villamil, Robert L. Shone
Abstract: The present invention relates to 5-fluoro-PGI.sub.2 derivatives of Formula I. These compounds are useful for the treatment of platelet dysfunction. Also disclosed is the process for preparing them and the appropriate intermediates.
Abstract: This invention relates to compounds having the formula ##STR1## wherein R.sub.1 represents hydrogen, halogen or alkoxy, R.sub.2 and R.sub.3 are hydrogen, alkanoyl or alkyl each being the same or different, R.sub.4 represents alkanoyloxyalkyl, hydroxyalkyl, hydrogen, alkyl, alkoxyalkyl, alkenyl, alkynyl, adamantanecarbonyloxyalkyl, bromoalkyl or benzoyloxyalkyl.