Abstract: A method of inhibiting the binding of PDGF using compounds of the formula I ##STR1## useful in the treatment of atherosclerosis, cancer, retinal detachment, pulmonary fibrosis, arthritis, psoriasis and glomerulonephritis, and restenosis following angioplasty or vascular surgery is disclosed.Also disclosed are pharmaceutical compositions and novel PDGF inhibitory compounds of the formula ##STR2## or a pharmaceutically acceptable addition salt thereof, useful in the treatment of atherosclerosis, cancer, retinal detachment, pulmonary fibrosis, arthritis, psoriasis and glomerulonephritis, and restenosis following angioplasty or vascular surgery.
Type:
Grant
Filed:
December 17, 1991
Date of Patent:
August 24, 1993
Assignee:
Schering Corporation
Inventors:
John W. Clader, Harry R. Davis, Deborra Mullins, Stuart Rosenblum, Jay Weinstein
Abstract: A synergistic antimicrobial composition comprising 2-alkyl-3-isothiazolones, preferably 4,5-dichloro-2-n-octyl-3-isothiazolone or 2-n-octyl-3-isothiazolone, and certain iodopropargyl compounds, in a ratio to each other which exhibits synergism is disclosed.
Abstract: Novel 1,3,2-benzodithiazole-1-oxides of formula (I) ##STR1## and their pharmaceutically acceptable salts are disclosed, wherein R.sup.1 is a substituent on the 4-, 5-, 6- or 7-position of the benzodithiazole nucleus selected from the group consisting of hydrogen, (C.sub.1 -C.sub.4)alkyl, halogen, halo(C.sub.1 -C.sub.4)alkyl, (C.sub.1 -C.sub.4)alkoxy, and nitro; andR.sup.2 is selected from the group consisting of (C.sub.1 -C.sub.12)alkyl; substituted (C.sub.1 -C.sub.12)alkyl; (C.sub.2 -C.sub.16)alkenyl; (C.sub.2 -C.sub.16)alkynyl; (C.sub.3 -C.sub.10)cycloalkyl; (C.sub.6 -C.sub.10)aryl; mono- or di-substituted (C.sub.6 -C.sub.10)aryl; (C.sub.6 -C.sub.10)aryl-(C.sub.1 -C.sub.4)alkyl; mono- or di-substituted (C.sub.6 -C.sub.10)aryl-(C.sub.1 -C.sub.4)alkyl; heterocycle-(C.sub.1 -C.sub.4)alkyl; and mono- or di-substituted heterocycle-(C.sub.1 -C.sub.4)alkyl.Also disclosed are the antifungal use and method of preparation of such compounds, as well as their formulation as pharmaceutical compositions.
Abstract: This invention relates to novel derivatives of tetralin, to the processes for their preparation, to their use as amino-peptidase inhibitors and to their end-use application as immunomodulators and as analgesic agents.
Abstract: The present invention relates to the compounds of formula (I). ##STR1## wherein R.sup.1 is C.sub.1-8 alkyl, C.sub.2-8 alkenyl, C.sub.5-8 cycloalkyl, aryl-C.sub.1-4 alkyl, aryl or heteroaryl; or aryl or heteroaryl which is mono-, di-, or trisubstituted independently with halogen, nitro, C.sub.1-4 alkyl, C.sub.1-4 alkoxy, trifluoromethyl, amino or C.sub.1-4 alkyl mono or disubstituted amino, pharmaceutical formulations containing these compounds and their use as vasodilators in the treatment of cardiovascular disorders.
Abstract: This invention relates to compounds of the formula ##STR1## where R.sub.1 and R.sub.2 are independently hydrogen or loweralkyl or R.sub.1 and R.sub.2 taken together with the carbon atom to which they are attached form a spiro-fused cycloalkane of 5 to 8 carbons; R.sub.3 and R.sub.4 are independently hydrogen or loweralkyl or R.sub.3 and R.sub.4 taken together with the carbon atom to which they are attached form a spiro-fused cycloalkane of 5 to 8 carbons; R.sub.5 and R.sub.6 taken together with the nitrogen atom to which they are attached are ##STR2## where X in each occurrence is independently hydrogen, halogen, loweralkyl, hydroxy, nitro, amino, cyano, trifluoromethyl or methoxy; and m is 0, 1 or 2; the pharmaceutically acceptable acid addition salts thereof and where applicable the optical and geometrical isomers and racemic mixtures thereof. The compounds of this invention are useful as analgesic and antihypertensive agents.
Abstract: Drug treatment therapies and kits for use therewith are disclosed. They involve the use of methimazole and/or its pro-drug carbimazole to reduce nephrotoxic effects of chemical exposure. In one embodiment, a patient receives cisplatin and then is treated with methimazole. The time delay in providing methimazole prevents the methimazole from being substantially expelled by the kidney prior to cisplatin reaching the kidney.
Abstract: Prodrugs of bio-active hydroxyaromatic drugs having the structural formula:A pharmaceutically acceptable prodrug of a biologically active, therapeutically effective hydroxyaromatic drug, said prodrug being selected from the group consisting of, (A) compounds having the structural formula:DRUG--O--CR'R"--Z].sub.nwherein:DRUG --O-- is the hydroxyaromatic O-dehydro residue of said drug;R' and R' may be the same or different and may be H, alkyl, aryl or electron withdrawing groups;Z is a displaceable leaving group; andn is an integer in the range of from 1 to 3, and (B) pharmaceutically acceptable salts thereof.
Abstract: This invention relates to 1-dimethylcarbamoyl-3-substituted-5-substituted-1H-1,2,4-triazoles of the formula ##STR1## wherein the substituents are as defined herein, compositions containing those compounds and methods of use.
Type:
Grant
Filed:
April 15, 1988
Date of Patent:
November 13, 1990
Assignee:
Rohm and Haas Company
Inventors:
Richard M. Jacobson, Luong T. Nguyen, Muthuvelu Thirugnanam
Abstract: The compounds: ##STR1## in which the dotted line represents optional unsaturation; R.sup.1 is hydrogen, halo or alkoxy; R.sup.2 is hydrogen or alkoxy and X is methylene, ethylene, ethylidene, 1,2-propylene or propylene; or a biologically acceptable salt thereof are growth promoting agents which rapidly lead to increased lean body mass in domestic animals and humans.
Abstract: This invention relates to novel [(substituted naphthalenyl)alkyl]-3H-1,2,3,5-oxathiadiazole 2-oxides, to the processes for their preparation, to methods for using the compounds, and to pharmaceutical compositions thereof. The compounds have pharmaceutical properties which render them beneficial for the treatment of diabetes mellitus and associated conditions.
Type:
Grant
Filed:
April 21, 1989
Date of Patent:
January 30, 1990
Assignee:
American Home Products Corporation
Inventors:
Thomas R. Alessi, Terence M. Dolak, John W. Ellingboe, Louis J. Lombardo
Abstract: This invention relates to novel benzyl-3H-1,2,3,5-oxathiadiazole 2-oxides, to the processes for their preparation, to methods for using the compounds, and to pharmaceutical preparations thereof. The compounds have pharmaceutical properties which render them beneficial for the treatment of diabetes mellitus and associated conditions.
Abstract: This invention relates to novel substituted 3H-1,2,3,5-oxathiadiazole 2-oxides, to the processes for their preparation, to methods for using the compounds, and to pharmaceutical compositions thereof. The compounds have pharmaceutical properties which render them beneficial for the treatment of diabetes mellitus and associated conditions.
Abstract: This invention relates to novel substituted 3H-1,2,3,5-oxathiadiazole 2-oxides, processes for their preparation, to methods for using the compounds, and to pharmaceutical preparations thereof. The compounds have pharmaceutical properties which render them beneficial for the treatment of diabetes mellitus and associated conditions.
Abstract: Novel insecticides of the formula ##STR1## in which n is 0 or 1,X is S, O, ##STR2## Y is N or ##STR3## Z is a 5- or 6-membered nitrogen-containing heterocyclic ring, and R to R.sup.9 variously represent hydrogen or specified organic radicals.
Abstract: The invention provides a method of combating a microorganism which comprises allowing a heterocyclic pentalene derivative of general formula I ##STR1## wherein X represents an oxygen atom, a sulphur atom or an --SO-- moiety; Y represents a sulphur, selenium or tellurium atom, provided that when Y represents a selenium or tellurium atom X is an oxygen atom; and R.sup.1 and R.sup.2 together represent a --CH.sub.2 --C(CH.sub.3).sub.2 --CCl(CONH.sub.2)-- or --CH.sub.2 --A--CH.sub.2 -- linkage where A is a --CH.sub.2 --, --CH(CH.sub.3)-- or --S(O).sub.n -- moiety, where n is 0, 1 or 2; provided that when X is an oxygen atom and Y is a sulphur atom R.sup.1 and R.sup.2 together represent a --CH.sub.2 --S(O).sub.n --CH.sub.2 -- linkage and when X is an --SO-- moiety and A is a S(O).sub.n --, n is 2; to act on the microorganism or its environment; and such derivatives for use as a therapeutic substance.
Abstract: The present invention relates to combating pests with five-membered nitrogen-containing heterocyclic compounds of the formula (I) ##STR1## in which R.sup.1, R.sup.2, R.sup.3, X and Y have the meaning given in the description. Many of the compounds are new.
Type:
Grant
Filed:
March 15, 1984
Date of Patent:
December 31, 1985
Assignee:
Bayer Aktiengesellschaft
Inventors:
Gerhard Jager, Rudolf Fauss, Kurt Findeisen, Benedikt Becker, Bernhard Homeyer