Abstract: There are provided 2-(p-chlorophenoxy) 2,2-dimethylacetate of /6'-(N-methylaminocarbonyloxymethyl) 2'-pyridyl/ methyl and its acid addition salts which have pharmacological properties particularly for regularizing metabolism, normalizing coagulation factors, combatting arteriosclerosis, chronic veinous insufficiencies and arterial hypertension. Also provided is a process for preparation of the compounds.
Abstract: The compounds are imidazo [1,2-a]pyridines which possess activity similar to histamine, in particular, they are agonists of H-1 histamine receptors. A compound of this invention is 2-(2-aminoethyl)imidazo [1,2-a]pyridine.
Type:
Grant
Filed:
July 31, 1975
Date of Patent:
July 20, 1976
Assignee:
Smith Kline & French Laboratories Limited
Abstract: The reaction between the alkali metal halopyridinates with the lower alkyl esters of .alpha.-chloro or bromo acetic acid (or propionic acid) to form the corresponding O-alkylated halopyridinates is catalyzed by quaternary ammonium salts. For example, methyl .alpha.-(6-chloropyridinyloxy)acetate was prepared in excellent yield by reacting sodium 6-chloropyridinate with excess methyl .alpha.-chloroacetate in the presence of 2 mole percent of benzyl triethyl ammonium chloride.
Abstract: A process for interrupting pregnancy is disclosed which comprises administration to a mammal an interceptive agent selected from a group of sulfonamidoaminopropiophenones. Illustrative of sulfonamidoaminopropiophenone interceptive agents useful in the process of the present invention for interrupting pregnancy are 4'-[3-(benzylmethylamino)propionyl]methanesulfonanilide and 4'-(3-hexamethyleniminopropionyl)methanesulfonanilide.
Abstract: Derivatives of 4-substituted phenyl 1,4-dihydropyridine 3,5-dicarboxylic acids substituted by lower alkyl groups in the 2- and 6-positions, are cardiovascular agents. The compounds, of which 2,6-dimethyl-4-[2-(diethylaminoethoxy)-phenyl]-1,4-dihydropyridine-3,5-dic arboxylic acid 3,5-diethyl ester is a typical example, can be prepared through condensation of a .beta.-dicarbonyl compound with an amine and an aldehyde, of an ylidene-.beta.-ketocarboxylic acid ester, with a .beta.-ketocarbonyl compound and an amine, of an aldehyde, an enamine and a .beta.-ketocarbonyl compound, or through elaboration of the substituent on the phenyl group.
Type:
Grant
Filed:
February 10, 1975
Date of Patent:
July 6, 1976
Assignee:
Bayer Aktiengesellschaft
Inventors:
Friedrich Bossert, Horst Meyer, Wulf Vater
Abstract: Orally effective, analgetic compositions have been developed which are useful in the prevention of drug abuse because upon parenteral administration, they do not produce analgesia, euphoria, or physical dependence. Such compositions comprise an orally active, strong analgetic in oral dosage form and containing, for each analgetic dose of the analgetic agent, an amount of naloxone sufficient, upon parenteral administration of said oral dosage form, to negate the analgetic, euphoretic and dependence producing action of the composition, but insufficient to block the therapeutic effect of the analgetic when the admixture is taken orally.
Abstract: 1,4-Dihydropyridines of the formula: ##SPC1##WhereinR is hydrogen, straight, branched or cyclic lower alkyl, lower alkenyl, or lower alkinyl, unsubstituted or substituted by hydroxyl or alkoxy of 1 to 3 carbon atoms; or benzyl, or phenethyl, unsubstituted or substituted in the aryl portion by 1 to 7 members selected from the group consisting of 1 to 3 alkoxy moieties of 1 to 3 carbon atoms, 1 or 2 alkyl moieties of 1 to 3 carbon atoms, and 1 or 2 halogen atoms;R.sub.1 is straight or branched chain alkyl of 1 to 4 carbon atoms;R.sub.
Abstract: Optically and therapeutically active compounds of the formula: ##SPC1##Wherein R represents a member selected from the group consisting of a straight or branched alkyl group of from one to twenty carbon atoms (C.sub.1 -C.sub.5 being preferred), an ethoxycarbonyl group, a benzyloxycarbonyl group, a phenyl group, an ##EQU1## group, wherein R is as defined above and R.sub.3 is a member selected from the group consisting of a hydrogen atom, a methyl group and a phenyl group, and a 2-, 3-, or 4-pyridyl group, or the HX salts thereof, wherein X represents a pharmaceutically acceptable acid addition salt anion, are prepared using optically active m-hydroxy-.alpha.-[(methylamino)-methyl]benzyl alcohol (phenylephrine).The compounds prepared by the process of this invention find therapeutic applicaton to warm-blooded animals (e.g., humans) in the management of asthma, nasal congestion and as decongestants, vasoconstrictors, mydriatic agents, and anti-glaucomatous agents in the practice of opthalmology.
Abstract: The invention pertains to indamines and salts thereof which are usefully employed in a dye composition for coloring keratinous fibers, especially human hair and in hair setting lotions which also includes a film-forming cosmetic resin.
Abstract: A series of novel 4-piperazino-6,7-dialkoxyquinazolines and 1-piperazino-6,7-dialkoxyisoquinolines have been prepared, including their acid addition salts. These compounds are useful in therapy as bronchodilators and as smooth muscle relaxants. Methods for their preparation from known compounds are provided.
Abstract: 3-Substituted-5-hydroxy(mercapto)alkylidene-rhodanine derivatives in which the 3-substituent is lower alkyl, cycloalkyl, alkenyl, phenyl, phenylalkyl, substituted phenyl or pyridylmethyl and having anti-arthritic activity are generally prepared from the appropriate 5-unsubstituted rhodanine by reaction with an orthoester followed by alkaline hydrolysis of the intermediate 5-alkoxyalkylidene rhodanine to give the 5-hydroxyalkylidene products or treatment of the intermediate rhodanine derivative with sodium sulfide to give the 5-mercaptoalkylidene products.
Abstract: Catechol amine solutions for physiological uses at mild pHs are provided, employing in combination a catecholalkyl amine, boric acid, a polyvinylpyrrolidone polymer and a physiologically acceptable antioxidant. The solutions are formulated in aqueous media and have greatly enhanced storage life, with substantially reduced susceptibility to light induced and oxidative degradation.
Abstract: Anti-allergic agents of ##EQU1## and heterocyclic oxamic acid derivation present the following formula: IN WHICHA is a member selected from the group consisting of 2-thiazolyl, 2-pyridyl, 2-pyridyl-N-oxide, 6-(lower)alkyl-2-pyridyl, 3-cyano-2-pyridyl, 3-pyridyl, 4-pyridyl, 2-pyrimidinyl, 2-pyrazinyl, .alpha.-naphthyl, .beta.
Type:
Grant
Filed:
January 20, 1975
Date of Patent:
June 29, 1976
Assignee:
American Home Products Corporation
Inventors:
John H. Sellstedt, Charles J. Guinosso, Albert J. Begany
Abstract: The C20 and C22 vinylogs of desmethyl retinoic acid have been found highly effective in promoting wound healing, in the treatment of acne, psoriasis and related skin disorders. The acid is applied to the site as a solution, ointment or powder. These acids are the most effective yet found for such purposes yet do not have some of the undesirable side effects of retinoic acid.
Type:
Grant
Filed:
October 29, 1974
Date of Patent:
June 29, 1976
Assignee:
The Regents of the University of California
Abstract: Novel compounds useful as antihistamine agents, antiallergy agents, and bronchodilators are represented by the following formula ##SPC1##Wherein R represents hydrogen or hydroxy; R.sup.1 represents hydrogen; or R and R.sup.1 taken together form a second bond between the carbon atoms bearing R and R.sup.1 ; n is a positive whole integer of from 1 to 3; Z represents thienyl, phenyl, or substituted phenyl wherein the substituents on the substituted phenyl may be attached at the ortho, meta, or para positions of the phenyl ring and are selected from halogen, a straight or branched lower alkyl chain of from 1 to 4 carbon atoms, a lower alkoxy group of from 1 to 4 carbon atoms, di(lower)alkylamino, or a saturated monocyclic heterocyclic group such as pyrrolidino, piperidino, morpholino, or N-(lower)alkylpiperazino. Pharmaceutically acceptable acid addition salts and individual optical isomers of compounds of the above formula are also included as a part of this invention.
Abstract: Novel compounds of formula 1 ##SPC1##And ##SPC2##Are useful in the prophylactic treatment of sensitized humans and animals for allergy and all anaphylactic reactions of a reagin or non-reagin mediated nature. The compounds are formulated with pharmaceutical carriers for oral, parenteral, inhalation or rectal means of administration.