Abstract: Compounds of the formula ##STR1## and the pharmaceutically acceptable, nontoxic, acid addition salts thereof, whereinR.sub.1 and R.sub.2 are each independently --H, lower alkyl, or cycloalkyl, with the proviso that R.sub.1 and R.sub.2 cannot both be --H or cycloalkyl at the same time;R.sub.1 and R.sub.2 taken together are cycloalkyl of 4-7 carbons;n is 0 or 1;X is (CH.sub.2).sub.2, CH.dbd.CH, or C.tbd.C;Y is independently selected from the group of --H, --Fl, --Br, --Cl, lower alkyl, and --OR.sub.3 ; wherein R.sub.3 is --H or lower alkyl; anda is 1 or 2, ortwo Y's taken together are --OCH.sub.2 O--;are useful as regulators of the cardiovascular system, particularly as hypotensive agents.
Abstract: A compound of the formula ##STR1## and the pharmaceutically acceptable acid addition salts thereof are potent antihypertensive agents and are therefore useful as cardiovascular system regulators.
Type:
Grant
Filed:
August 29, 1983
Date of Patent:
September 24, 1985
Inventors:
Joseph M. Muchowski, Robert Greenhouse, Jack Ackrell, Tsung-Tee Li, Jurg R. Pfister
Abstract: A compound represented by the formula ##STR1## wherein R.sup.1 is an alkali metal cation or hydrogen and which useful for increasing the feed efficiency of ruminants and for treating coccidiosis in domestic animals, especially chickens.
Abstract: Compounds of the formula: ##STR1## and the pharmaceutically acceptable acid addition salts thereof, wherein; Y is halo, alkoxy, alkyl, or dialkylamino;a is 0, 1 or 2;b is an integer from 2-12 with the proviso that if b is 2 or 3 a cannot be 0; andX is selected from the group consisting of: --OH, OR.sup.1, --NH.sub.2, --NHR.sup.1, NR.sub.2.sup.1, ##STR2## and --NHCONHR.sup.2 in which each R.sup.1 is independently alkyl or cycloalkyl or in --NR.sub.2.sup.1, both R.sup.1 together are alkylene or form a piperazine ring optionally substituted at the ring N by alkyl or --CH.sub.2 CH.sub.2 OH; andR.sup.2 is alkyl, cycloalkyl, or optionally substituted phenyl;have antiinflammatory properties and are useful in the treatment of conditions characterized by inflammation and swelling.
Type:
Grant
Filed:
January 9, 1984
Date of Patent:
August 20, 1985
Assignee:
Syntex (U.S.A.) Inc.
Inventors:
Peter H. Nelson, Howard J. Ringold, Stefan H. Unger, Thomas R. Thieme
Abstract: Compounds of the formula: ##STR1## and the pharmaceutically acceptable, non-toxic salts and esters (alkyl, 1-6C) thereof, wherein:X is O or S;R.sup.1 is selected from the group consisting of:(a) alkyl or cycloalkyl of 3-8 carbons,(b) ##STR2## in which Z is O, S or --CH.sub.2, and Y is lower alkyl (1-4C), lower alkoxy (1-4C), halo, or --CF.sub.3, and(c) ##STR3## in which Z and X are as herein defined; and R.sup.2 is hydrogen or methyl;exhibit prostaglandin-like activity and are, thus, useful as platelet aggregation inhibitors.
Abstract: A method for removing trace amounts of contaminating hydrazine from pharmaceutical grade PVP. An aqueous solution of PVP is contacted with a gaseous stream containing ozone for a period of time sufficient to remove the hydrazine.
Abstract: Synthetic nonapeptide and decapeptide LHRH agonists analogs having a novel gaunadino-substituted, amidine, tertiary or quatrinary aminoacyl residue at position 6 are disclosed herein.
Abstract: Compounds of the formula: ##STR1## and the pharmaceutically acceptable acid addition salts thereof, wherein: Z is S;Y is halo, alkoxy, alkyl, or dialkylamino;a is 0, 1 or 2;b is an integer from 2-12 with the proviso that if b is 2 or 3, a cannot be 0, and with the further proviso that if X is OH, b cannot be 2-5 and with the further proviso that if X is --NH.sub.2, b cannot be 2-5; andX is selected from the group consisting of: --OH, OR.sup.1, --NH.sub.2, --NHR.sup.1, NR1/2, ##STR2## and --NHCONHR.sup.2 in which each R.sup.1 is independently alkyl or cycloalkyl or, in --NR1/2, both R.sup.1 s together are alkylene or form a piperazine ring optionally substituted at the ring N by alkyl or --CH.sub.2 CH.sub.2 OH; andR.sup.2 is alkyl, cycloalkyl, or optionally substituted phenyl;have antiinflammatory properties and are useful in the treatment of conditions characterized by inflammation and swelling.
Type:
Grant
Filed:
February 18, 1982
Date of Patent:
April 23, 1985
Assignee:
Syntex (U.S.A.), Inc.
Inventors:
Peter H. Nelson, Howard J. Ringold, Stefan H. Unger, Thomas R. Thieme
Abstract: 5-benzoyl-7-halo-1,2-dihydro-3H-pyrrolo[1,2-a]-pyrrole-1-carboxylic acids, represented by the formula ##STR1## and the pharmaceutically acceptable non-toxic esters and salts thereof, wherein:R is hydrogen or lower alkyl;X is hydrogen, lower alkyl, lower alkoxyl, lower alkoxycarbonyl, carboxyl, lower alkylcarbonyl, sulfonic acid, sulfonic acid alkyl ester, fluoro, chloro, or bromo; and Y is chloro or bromo, which are novel, and 5-benzoyl-1,2-dihydro-3H-pyrrolo[1,2-a]pyrrole-1-carboxylic acids which are represented by the formula ##STR2## wherein X and R are as above defined except that X cannot be chloro or bromo, are prepared by decarboxylation of the corresponding 1,1 dicarboxylates. Intermediates in said preparation are also disclosed.
Abstract: Novel compounds of the general formula: ##STR1## and the pharmaceutically acceptable acid addition salts thereof, wherein: R.sup.1, R.sup.2, R.sup.3 and R.sup.4 are each independently hydrogen, lower alkyl, lower alkoxy, trifluoromethyl, halo, lower alkylthio, lower alkyl sulfinyl or lower alkyl sulfonyl;R.sup.5 is hydrogen or lower alkyl;m is 0 or 1;W is alkylene, --CH.dbd.CH--, --O--, or --N(R.sup.6)--, where R.sup.6 is lower alkyl or hydrogen;n is 0 or 1; andQ is lower alkyl, cycloalkyl or optionally substituted phenyl.These compounds combine .beta.-blockade and calcium entry blockade properties in the same compound and therefore are useful in therapy in the treatment of cardiovascular diseases, including myocardial infarction, hypertension, arrhythmia and variant and exercise induced angina. The compounds are also useful in immunosuppressant therapy for immune diseases, such as rheumatoid arthritis.
Abstract: 2-(1,4-Benzodioxan-2-ylalkyl)imidazoles having the general formula: ##STR1## wherein R.sup.1, and R.sup.2 and R.sup.3 are independently selected from the group consisting of hydrogen, and alkyl (1-6C), and wherein n is an integer equal to 0, 1 or 2, and the pharmaceutically acceptable acid addition salts thereof, are .alpha..sub.2 blockers and thus are useful as affectors of the CNS, specifically as platelet aggregation inhibitors and as antihypertensives.
Type:
Grant
Filed:
August 5, 1981
Date of Patent:
February 5, 1985
Assignee:
Syntex (U.S.A.) Inc.
Inventors:
Arthur F. Kluge, Arthur M. Strosberg, Roger L. Whiting, George A. Christie
Abstract: Novel compounds of this invention are tetrazole, acylhydroxylamine, hydroxymethylketone and amide derivatives of unsaturated fatty acids which are selective inhibitors of the enzymes lipoxygenase and cyclooxygenase involved in the production of pain, inflammation, bronchoconstriction and allergic reactions. These compounds are beneficial in the treatment of a number of inflammatory and/or painful conditions and allergic reactions.
Abstract: This invention concerns the novel use of certain known thiazoles, particularly acylaminothiazoles and thiazolecarboxamides, as intraocular pressure lowering agents. When administered topically to the eye with increased intraocular pressure the compounds are effective in decreasing intraocular pressure, in preventing development of acute or chronic ocular hypertension including glaucoma, in inhibiting the further deterioration of the eye due to intraocular hypertension, or in relieving the symptoms of already existing ophthalmic disease.
Type:
Grant
Filed:
October 19, 1982
Date of Patent:
October 16, 1984
Assignee:
Syntex (U.S.A.) Inc.
Inventors:
L. David Waterbury, A. Peter Roszkowski
Abstract: The present invention concerns a new use of certain pyrrolo-pyrrole compounds of chemical formulas (A), (B), (C), and (D): ##STR1## for the treatment of microvascular complications associated with diabetes such as, for example, diabetic retinopathy, diabetic nephropathy and diabetic neuropathy. Pyrrolo-pyrrole compounds prevent development, restrain further progress and relieve symptoms of already developed microvascular complications of diabetes.
Abstract: 5-Substituted-1,2-dihydro-3H-pyrrolo[1,2-a]pyrrole-1-carboxylic acids of the formula ##STR1## wherein: X is hydrogen or lower alkyl; Ar is a moiety selected from the group consisting of ##STR2## in which: Y is oxygen or sulfur;R is hydrogen, methyl, chloro, or bromo, the R substitution being at the 3, 4 or 5 position of the ring;R.sup.1 is hydrogen, lower alkyl, lower alkoxyl, lower alkoxycarbonyl, lower alkylcarbonyl, fluoro, chloro or bromo, the R.sup.1 substitution being at any available position in the ring;R.sup.2 is hydrogen or lower alkyl;are prepared by .beta.-decarboxylation of the corresponding dialkyl-1,1-dicarboxylates. Certain substituted pyrroles are useful as intermediates for preparing the compounds of formula I.
Abstract: 5-benzoyl-7-halo-1,2-dihydro-3H-pyrrolo[1,2-a]-pyrrole-1-carboxylic acids, represented by the formula ##STR1## and the pharmaceutically acceptable non-toxic esters and salts thereof, wherein:R is hydrogen or lower alkyl;X is hydrogen, lower alkyl, lower alkoxyl, lower alkoxycarbonyl, carboxyl, lower alkylcarbonyl, sulfonic acid, sulfonic acid alkyl ester, fluoro, chloro, or bromo; and Y is chloro or bromo, which are novel, and 5-benzoyl-1,2-dihydro-3H-pyrrolo[1,2-a]pyrrole-1-carboxylic acids which are represented by the formula ##STR2## wherein X and R are as above defined except that X cannot be chloro or bromo, are prepared by decarboxylation of the corresponding 1,1 dicarboxylates. Intermediates in said preparation are also disclosed.
Abstract: 5-Substituted-1,2-dihydro-3H-pyrrolo[1,2-a]pyrrole-1-carboxylic acids of the formula ##STR1## wherein: X is hydrogen, lower alkyl, chloro or bromo; Ar is a moiety selected from the group consisting of ##STR2## in which: Y is oxygen or sulfur;R is hydrogen, methyl, chloro, or bromo, the R substitution being at the 3, 4 or 5 position of the ring;R.sup.1 is hydrogen, lower alkyl, lower alkoxyl, lower alkoxycarbonyl, lower alkylcarbonyl, fluoro, chloro or bromo, the R.sup.1 substitution being at any available position in the ring;R.sup.2 is hydrogen or lower alkyl;are prepared by .beta.-decarboxylation of the corresponding dialkyl-1,1-dicarboxylates. Certain substituted pyrroles are useful as intermediates for preparing the compounds of formula I.
Abstract: Certain known pyrroles have been found to be useful in the topical treatment of various ophthalmic diseases in mammals; especially those originating from or associated with inflammation such as, for example, cystoid macular edema, glaucoma, conjunctivitis, uveitis, diabetic retinopathy and eye surgery or trauma.
Abstract: Delivery systems for releasing macromolecular active agents to a body site at a controlled rate for a prolonged period of time, comprising a cholesteric matrix permeable to passage of the macromolecular active agent by diffusion, are disclosed. The cholesteric matrix comprises cholesterol powder and cholesterol prills optionally in combination with a binding agent and a lubricating agent. The macromolecular active agent is dispersed throughout the matrix; macromolecules suitable for release from this delivery system have molecular weights of about 1300 to about 75,000 and are at least very slightly soluble in water.