Abstract: Tricyclic antidepressant functionalized compounds are provided for conjugation through a side chain to antigenic compounds, particularly poly(amino acids), and enzymes. The antigenic conjugates are employed for the production of antibodies and together with the enzyme conjugates find particular use in immunoassays for the determination or detection of the total amount of tricyclic antidepressants present in a sample.
Type:
Grant
Filed:
August 21, 1986
Date of Patent:
September 20, 1988
Assignee:
Syntex (U.S.A.) Inc.
Inventors:
Christine G. Collins, Marcel R. Pirio, Prithipal Singh
Abstract: Circulation-active dihydropyridines of the formula ##STR1## in which R.sup.1 is optionally substituted aryl or heterocyclic,R.sup.2 is H, NO.sub.2, CN, C.sub.1 -C.sub.8 -alkylsulphonyl, aryl or carboalkoxy,R.sup.3 is alkyl or aryl,R.sup.4 is H or alkyl,X is C.dbd.O or a direct bond, andn is a number from 1 to 20,or physiologically acceptable salts thereof. A synthesis using morpholines or thiomorpholines is also disclosed.
Type:
Grant
Filed:
July 25, 1986
Date of Patent:
September 6, 1988
Assignee:
Bayer Aktiengesellschaft
Inventors:
Horst Meyer, Gerhard Franckowiak, Gunther Thomas, Matthias Schramm, Michael Kayser, Martin Bechem, Rainer Gross
Abstract: This invention provides novel alkane derivatives which are leukotriene antagonists, formulations of those derivatives, and a method of using those derivatives for the treatment of conditions characterized by an excessive release of leukotrienes.
Abstract: Compounds of the formula ##STR1## wherein R.sub.1 is hydrogen or alkyl of 1 to 4 carbon atoms;R.sub.2 is 2-, 3- or 4-pyridyl, phenyl or mono- or di- substituted phenyl, where the substituents are each individually alkoxy of 1 to 2 carbon atoms, fluorine, chlorine, bromine, trifluoromethyl, alkyl or 1 to 4 carbon atoms, hydroxyl or nitro; andR.sub.3 and R.sub.4 are each independently hydrogen or alkyl of 1 to 4 carbon atoms; orR.sub.3 and R.sub.4, together with each other and the nitrogen atom to which they are attached, form an unsubstituted or methyl-substituted, saturated 5- or 6-membered heterocycle which may contain an additional oxygen or nitrogen heteroatom, or form an imidazole ring;where the aminomethyl substituent is attached to the 4- or 5-position or the pyrrolidine ring, and non-toxic, pharmacologically acceptable acid addition salts thereof. The compounds as well as the salts are useful as nootropics and antihypoxics.
Type:
Grant
Filed:
June 26, 1986
Date of Patent:
August 30, 1988
Assignee:
Boehringer Ingelheim KG
Inventors:
Karl-Heinz Weber, Gerhard Walther, Claus Schneider, Dieter Hinzen, Franz J. Kuhn, Erich Lehr
Abstract: An RDX-HMX mixture containing a major amount of RDX is separated into essially pure RDX and essentially pure HMX by first treating the mixture with DMSO to dissolve all the HMX present then recovering the remaining undissolved RDX as an essentially pure material. The dissolved mixture which contains a major amount of HMX and a minor amount of RDX is treated with cyclohexanone to dissolve all the RDX present, then the undissolved HMX remaining in the liquor is recovered as an essentially pure material.
Type:
Grant
Filed:
November 7, 1986
Date of Patent:
August 30, 1988
Assignee:
The United States of America as represented by the Secretary of the Army
Abstract: The invention is concerned with novel heterocyclic compounds of the formula ##STR1## wherein R is C.sub.1-12 -alkyl, C.sub.3-12 -alkenyl, C.sub.3-12 -alkynyl or C.sub.3-8 -cycloalkyl and X signifies oxygen or sulfur, and none of the possible multiple bonds of R is present in the .alpha.-position to X, and their acid addition salts, processes for their manufacture, insect control compositions which contain these compounds as the active substance as well as the use of such compounds or compositions for the control of insects. Moreover, the invention is concerned with starting materials used for the preparation of such compounds.
Abstract: The present invention relates to novel methods for the preparation of quinoline-2,3-dicarboxylic acid, useful for the preparation of the highly effective 2-(2-imidazolin-2-yl)quinoline-3-carboxylic acid herbicidal agents.
Abstract: The present invention is novel 2-isopropoxy-N-1H-tetrazol-5-yl-benzamides having unexpected inhibition of histamine release from human basophils.
Abstract: This invention provides novel compounds which are leukotriene antagonists, certain novel intermediates to the compounds, formulations of the compounds, and a method of using the compounds for the treatment of conditions characterized by an excessive release of leukotrienes.
Abstract: Compounds of the formula: ##STR1## where R is hydrogen or A--(CF.sub.2).sub.m --CH.sub.2 --; A is --F or --H; n is an integer from 1 to 10, inclusive; m is an integer from 0 to 9, inclusive; p is an integer from 0 to 4, inclusive; and Y is hydrogen, halo, trifluoromethyl, alkyl of 1 to 6 carbon atoms, alkoxy of 1 to 6 carbon atoms, or hydroxy; or a pharmaceutically acceptable salt thereof. The compounds are useful as anti-hyperglycemic and anti-hyperinsulinemic agents.
Abstract: A novel quinaldinamide derivative having the formula: ##STR1## wherein each of R.sup.1 and R.sup.2 independently represents a lower alkyl group or R.sup.1 and R.sup.2 are combined together with the adjacent nitrogen atom to form a 5-7 membered ring; and X represents the hydrogen atom, a lower alkyl group or a lower alkoxy group, and its acid-addition salt, which show prominent central muscle relaxant effect, namely rigidity relieving effect on anemic decerebrated rigidity.
Abstract: A novel class of diaminoether compounds wherein one amino group thereof is a tertiary amine in N-heterocyclic form and the other amino group is a severely sterically hindered secondary amino group may be prepared by a three-step process and are useful in the selective removal of H.sub.2 S from mixtures containing H.sub.2 S and CO.sub.2.
Abstract: Compounds of formula (1) ##STR1## wherein A and B are identical or different alkyl, aralkyl or cycloalkyl groups or carbocyclic or heterocyclic aromatic radicals, R.sub.1 and R.sub.2 are hydrogen atoms or substituents which do not impart solubility in water, are particularly suitable as photoconductive substances.
Type:
Grant
Filed:
August 29, 1986
Date of Patent:
July 26, 1988
Assignee:
Ciba-Geigy Corporation
Inventors:
Alain C. Rochat, Abul Iqbal, Remy Jeanneret, Jin Mizuguchi
Abstract: There is described the use of pyrrothine derivatives of the general formula I ##STR1## wherein R.sub.1 and R.sub.3 signify hydrogen or methyl, R.sub.2 hydrogen, methyl or an acyl group with 1 to 5 carbon atoms and X and Y signify hydrogen, an equivalent of a physiolgically acceptable cation or together a single bond, for the inhibition of the allergen-induced degranulation of peripheral leukocytes.
Type:
Grant
Filed:
May 15, 1986
Date of Patent:
July 26, 1988
Assignee:
Boehringer Mannheim GmbH
Inventors:
Peter Stahl, Hans Seidel, Herbert Von der Eltz, Otto-Henning Wilhelms, Androniki Roesch
Abstract: The invention relates to new N-cyclic benzenesulfonamides, their process of preparation and their use as active substance of pharmaceutical compositions. The new benzenesulfonamides according to the invention correspond to the following general formula (I): ##STR1## in which: V represents, for example, hydrogen,W represents, for example CF.sub.3,X represents, for example, hydrogen,Y represents, for example, hydrogen,n is 2 or 3,Z represents, for example, the group NR.sub.4, in which R.sub.4 represents, for example, hydrogen.These compounds are useful in pharmaceutical compositions for the treatment of nervous disorders with anxiety.
Type:
Grant
Filed:
October 18, 1984
Date of Patent:
July 26, 1988
Assignee:
DROPIC, Societe Civile de gestion de droits de Propriete Industrielle
Inventors:
Pierre Roger, Patrick Choay, Jean-Paul Fournier
Abstract: There is disclosed a process for the preparation of 2-(imidazolin-2-yl)-3-pyridine and -3-quinolinecarboxylic acids of formula ##STR1## wherein R.sub.1 is hydrogen or C.sub.1 -C.sub.4 alkyl, R.sub.2 is hydrogen, halogen, C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 hydroxyalkyl, C.sub.1 -C.sub.4 alkoxy, phenyl or phenyl-C.sub.1 -C.sub.4 alkyl, or phenyl or phenyl-C.sub.1 -C.sub.4 -alkyl, each substituted by one C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy or halogen, R.sub.3 is hydrogen, C.sub.1 -C.sub.4 alkyl, phenyl, phenyl-C.sub.1 -C.sub.4 -alkyl, or phenyl or phenyl-C.sub.1 -C.sub.4 -alkyl, each substituted by one C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy or halogen, R.sub.2 and R.sub.3 together are 1,3-butadienylene which can be substituted by halogen, C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy, C.sub.1 -C.sub.4 haloalkyl, C.sub.1 -C.sub.4 alkylsulfonyl, nitro, cyano, phenyl, phenoxy, or phenyl or phenoxy, each substituted by one C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.
Abstract: Indolyl dieneoic acids and esters are disclosed possessing valuable pharmaceutical activity, particularly as lipoxygenase inhibitors with anti-inflammatory and anti-allergic properties.
Type:
Grant
Filed:
January 21, 1986
Date of Patent:
July 19, 1988
Assignee:
USV Pharmaceutical Corp.
Inventors:
Wan-kit Chan, Thomas D. Lee, Fu-chih Huang
Abstract: The invention relates to new coenzyme A and N-hydroxysuccinimidyl esters of all-trans- and 13-cis-retinoic acid and to methods for preparing the same. A new method for preparing all-trans-retinoic acid anhydride is also disclosed.
Type:
Grant
Filed:
June 2, 1986
Date of Patent:
July 12, 1988
Assignee:
Wisconsin Alumni Research Foundation
Inventors:
Hector F. DeLuca, Andrzej Kutner, Heinrich K. Schnoes
Abstract: The present invention relates to novel methods for the preparation of quinoline-2,3-dicarboxylic acid, useful for the preparation of the highly effective 2-(2-imidazolin-2-yl)quinoline-3-carboxylic acid herbicidal agents.