Abstract: N.sup.6 -acenaphthyl adenosines and analogs thereof and pharmaceutically acceptable acid addition salts having highly desirable blood pressure lowering properties, processes for their manufacture and pharmaceutical compositions and methods for using said compounds and compositions are described.
Type:
Grant
Filed:
September 5, 1985
Date of Patent:
September 30, 1986
Assignee:
Warner-Lambert Company
Inventors:
Harriet W. Hamilton, William C. Patt, Bharat K. Trivedi
Abstract: Liposomes of steryl glucosides and/or steryl glucoside monopalmitates are useful for hemostatic, vascular stabilization and anti-shock effects, particularly in the form of injectable solutions.
Abstract: Process for production of tea catechins selected from (-) epicatechin, (-) epigallocatechin, (-) epicatechin gallate and (-) epigallocatechin gallate comprising extracting tea leaves with hot water or an aqueous solution of methanol, ethanol or acetone, washing the extract containing solution with chloroform, transferring the washed solution into an organic solvent, removing the solution and passing the resulting solution through a reversed phase column in the presence of an eluting solution. Tea catechins and methods of using the same are also disclosed.
Abstract: A remedial or prophylactic agent for the treatment of obstructive respiratory diseases comprises a therapeutically effective amount of L-fucose.
Abstract: Compounds of the formula ##STR1## in which R.sup.1 is hydrogen, halogen or alkyl,R.sup.2 is halogen, alkyl or alkylthio,X is oxygen or sulphur, andY is hydrogen, halogen, alkyl or halogenoalkyl,which possess pesticidal activity.
Type:
Grant
Filed:
June 13, 1983
Date of Patent:
September 9, 1986
Assignee:
Bayer Aktiengesellschaft
Inventors:
Albrecht Marhold, Wilhelm Sirrenberg, Erich Klauke, Ingeborg Hammann, Benedikt Becker, Ingomar Krehan, Wilhelm Stendel
Abstract: Process for preparing esters of 2-(6'-methoxy-2'-naphtyl)-propionic acid via rearrangement of new ketals of 2-halo-1-(6'-methoxy-2'-naphtyl)-propan-1-one in the presence of a Lewis acid.The esters thus obtained are useful as intermediate products for preparing Naproxen.
Type:
Grant
Filed:
May 17, 1985
Date of Patent:
September 2, 1986
Assignee:
Blaschim S.p.A.
Inventors:
Claudio Giordano, Aldo Belli, Fulvio Uggeri, Giovanni Villa
Abstract: A process for the production of the beetle aggregation pheromone brevicomin comprising reacting acrolein dimer sequentially with ethyllithium, a methylating agent and aqueous protonic acid. In a modification of the process the acrolein dimer is reacted with ethyl Grignard reagent prior to reaction with an alkyllithium compound. The process includes distributing the brevicomin product to areas to be controlled for beetles.
Abstract: 5-fluoro-2'-deoxyuridine derivatives expressed by general formula (1) and their pharmacologically permissible salts ##STR1## wherein A indicates a saturated or unsaturated divalent aliphatic hydrocarbon group having 1 to 30 carbon atoms; the letter n indicates 0 or 1, and when n is 0, it indicates that Y is directly bound to an oxygen atom; Y represents a hydrogen atom, phenyl group, or substituted phenyl group; however, when Y is a hydrogen atom, n is 1; R indicates a hydrogen atom or alcohol-protecting group.These compounds have a very strong antitumor activity.
Abstract: This disclosure describes the preparation of 3'-amino-2',3'-dideoxycytidine and the pharmacologically acceptable salts thereof which are useful in inhibiting the growth of transplanted tumors in mammals.
Abstract: A surfactant having the capacity of reducing the surface tension in pulmonary alveoli significantly is provided. The surfactant consists essentially of, based on the total weight of the surfactant, 50.6-85.0% of a chlorine phosphogylceride, 4.5-37.6% of an acid phospholipid, 4.6-24.6% of a fatty acid or its analogue and 0.1-10.0% of a lipoprotein derived from the lung of a mammal. These components cooperate to form a kind of film at a gas-liquid interface within pulmonary alveoli and reduce the surface tension. A pharmaceutical composition comprising the surfactant is useable for the clinical treatment of respiratory distress syndrome.
Abstract: Cyclohexane-1,3-dione derivatives of the formula ##STR1## where R.sup.1 is alkyl, R.sup.2 is alkyl, unsubstituted or halogen-substituted alkenyl or alkynyl, X is a saturated or unsaturated five-membered or six-membered heterocyclic structure which carries one or more substituents, and Z is hydrogen, methoxycarbonyl, ethoxycarbonyl, methyl or cyano, and salts of these compounds are used for controlling undesirable plant growth.
Type:
Grant
Filed:
July 6, 1984
Date of Patent:
July 29, 1986
Assignee:
BASF Aktiengesellschaft
Inventors:
Rainer Becker, Dieter Jahn, Michael Keil, Walter Himmele, Bruno Wuerzer
Abstract: The present invention relates to novel compounds and processes. In particular, the invention relates to novel analogs of the aminocyclitol antibiotic spectinomycin. More particularly, it relates to novel processes for synthesizing analogs of spectinomycin; both known analogs and the novel analogs of the present invention. Additionally, the invention includes novel intermediates.The novel analogs of spectinomycin disclosed herein are useful as antimicrobial agents.
Abstract: This invention relates to new products of the general formula ##STR1## where R.sub.1 =H, OH, OCOCH.sub.3, OSO.sub.2 CH.sub.3, branched or unbranched alkyl containing 1 to 5 carbon atoms. R.sub.2 =NHCOR.sub.3, NHCOCH.sub.2 X, NHSO.sub.2 CH.sub.3, N(SO.sub.2 CH.sub.3).sub.2, SO.sub.2 N(CH.sub.3).sub.2, SO.sub.2 NHCH.sub.3, SO.sub.2 NCH.sub.3 CH.sub.2 CH.sub.2 OH, SO.sub.2 NH.sub.2 wherein R.sub.3 is a lower alkyl containing 1 to 4 carbon atoms; and X is NR.sub.4 R.sub.5 or ##STR2## wherein R.sub.4 and R.sub.5 are both independently lower alkyls containing 1 to 4 carbon atoms and ##STR3## is piperidine, pyrrolidine or morpholine. These products can be in the form of pharmaceutically acceptable derivatives such as esters, amides, salts. When R.sub.2 contains an amino function, the product can be in the form of an acid salt.These products are prepared from their methyl esters either by reaction between ##STR4## and paramethoxycarbonylbenzoic acid chloride or by means of derivative I such as R.sub.2 is NH.sub.2.
Type:
Grant
Filed:
March 22, 1984
Date of Patent:
July 15, 1986
Assignee:
Societe Cortial, S.A.
Inventors:
Marie-Helene Creuzet, Claude Feniou, Francoise Guichard, Gisele Prat, Jacqueline Mosser, Henri Pontagnier
Abstract: Aromatic compounds which contain perfluorinated side-chains bonded via a heteroatom are prepared by treating aromatic compounds, which contain side-chains which are perhalogenated, but only partially fluorinated, and bonded via heteroatom, with a catalyst capable of transferring halogen atoms.
Abstract: The invention relates to novel benzodioxole derivatives of the general formula I ##STR1## in which R.sub.1 represents an unsubstituted or substituted, aliphatic, aromatic or heteroaromatic radical,alk represents an alkylene, alkenylene or alkylidene radical having a maximum of 5 carbon atoms,n.sub.1 represents 0, 1 or 2n.sub.2 represents 0 or 1,R.sub.2, R.sub.3 and R.sub.4 each represents, independently of the others, hydrogen, lower alkyl, lower alkoxy or halogen, andA represents the radical --O--R.sub.5, wherein R.sub.5 represents hydrogen or an unsubstituted or substituted, aliphatic or araliphatic hydrocarbon radical, or A represents the radical ##STR2## in which either R.sub.6 and R.sub.7 each represents, independently of the other, hydrogen or lower alkyl, or R.sub.6 and R.sub.
Abstract: Benzothien-3-yl adenosine; benzothien-3-yl adenosine, S-oxide; and benzothien-3-yl adenosine, S,S-dioxide compounds or pharmaceutically acceptable acid addition salts having highly desirable central nervous system and antihypertensive properties, processes for their manufacture and pharmaceutical compositions and methods for using said compounds and compositions are described.
Abstract: 2,6-di-O-methyl-beta-cyclodextrin complexes of compounds of the formula (1a) ##STR1## wherein R.sup.2' stands for C.sub.1 to C.sub.12 alkyl or a group of the formula ##STR2## in which R.sup.11 is C.sub.1 to C.sub.4 alkyl;R.sup.12 is hydrogen or C.sub.1 to C.sub.4 alkyl;n is 0 or 1;p is 1 to 4;r is 1 to 4; andR.sup.3' and R.sup.4' are each C.sub.1 to C.sub.4 alkyl, or pharmaceutically salts thereof are disclosed, having analgesic activity.
Type:
Grant
Filed:
December 2, 1983
Date of Patent:
July 8, 1986
Assignee:
Chinoin Gyogyszer es Vegyeszeti Termekek Gyara RT
Abstract: The present invention relates to new condensed benzopyrone derivatives, to a process for their preparation and to pharmaceutical compositions containing them.
Type:
Grant
Filed:
March 22, 1984
Date of Patent:
July 1, 1986
Assignee:
Farmitalia Carlo Erba, S.p.A.
Inventors:
Gianfederico Doria, Carlo Passarotti, Ada Buttinoni
Abstract: Benzyl esters of the formula ##STR1## in which n is 1,2,3,4, or 5,R.sup.2 is hydrogen, C.sub.1-4 -alkyl, cyano or ethynyl,R.sup.3 is the radical of a carboxylic acid customary in pyrethroids or pyrethroid-like compounds, andat least one R.sup.1 is fluoroalkoxy or fluoroalkylmercapto, or two together are fluoromethylene- or fluoroethylene-dioxy, and the others, if present, are hydrogen or various radicals,which possess arthropodicidal properties. Various alcohols, amines, aldehydes, halides, and the like, corresponding to the alcohol moieties of the esters are also synthesized.
Type:
Grant
Filed:
November 2, 1983
Date of Patent:
June 24, 1986
Assignee:
Bayer Aktiengesellschaft
Inventors:
Reinhard Lantzsch, Albrecht Marhold, Wolfgang Behrenz, Ingeborg Hammann
Abstract: The administration of sex hormones, particularly testosteorne, progesterone and estradiol in the form of their complexes or inclusions with specific derivatives of cyclodextrins by the sublingual or buccal route results in effective transfer of these hormones into the systemic circulation, followed by only gradual elimination. To be effective in the above mode of administration, the derivatives of cyclodextrins must carry one or several substituents, each containing one or several hydroxy groups. Specially preferred are the following complexes: hydroxypropylbeta-cyclodextrin and poly-beta-cyclodextrin.
Type:
Grant
Filed:
April 25, 1984
Date of Patent:
June 24, 1986
Assignee:
The United States of America as represented by the Secretary, Dept. of Health & Human Services