Abstract: The use of nicotinic anilide derivatives of the general formula ##STR1## where the substituents have the following meanings: R.sup.1 halogen, methyl, trifluoromethyl, methoxy, methylthio, methylsulfinyl, methylsulfonylR.sup.2 unsubstituted or halogen-substituted alkyl, unsubstituted or halogen-substituted alkenyl, alkynyl, unsubstituted or halogen-substituted alkoxy, unsubstituted or halogen-substituted alkenyloxy, alkynyloxy, cycloalkyl, cycloalkenyl, cycloalkyloxy, cycloalkenyloxyfor combating Botrytis, and nicotinic anilides of the formula I.
Type:
Grant
Filed:
June 7, 1995
Date of Patent:
December 31, 1996
Assignee:
BASF Aktiengesellschaft
Inventors:
Karl Eicken, Norbert Goetz, Albrecht Harreus, Eberhard Ammermann, Gisela Lorenz, Harald Rang
Abstract: The present invention relates to a novel compound having a 12-lipoxygenase inhibitory effect, of the general formula (I), a precursor thereof, and a medicine containing the same, ##STR1## wherein R.sup.1 represents a hydrogen atom or a hydroxy group; one of R.sup.2 and R.sup.3 represents a hydrogen atom, while the other cyano group ; and Ar is a group represented by the following general formula (a), (b) or (c), ##STR2## wherein R.sup.4 represents a hydrogen atom, a lower alkyl group, a lower alkoxy group, a halogen atom, a thrifluoromethyl group or a cyano group.
Abstract: The invention relates to 7-[5-hydroxy-2-(hydroxyhydrocarbyl or heteroatom-substituted hydroxy hydrocarbyl)-3-hydroxycyclopentyl(enyl)] heptanoic or heptenoic acids and derivatives of said acids, wherein one or more of said hydroxy groups are replaced by an ether group. The compounds of the present invention are potent ocular hypotensives, and are particularly suitable for the management of glaucoma.
Abstract: Novel bis-sulfonium salts of amino substituted bis(halomethyl)benzene are disclosed. The sulfonium salts are prepared by reaction of an amino substituted bis(halo methyl)benzene with an aliphatic sulfide. These sulfonium salts can be made into polymer having non-linear optical properties, and polymers which can be converted to electrically conductive polymers. Such polymers are produced by reacting a novel bis-cycloalkylene sulfonium salt of 2,5,N,N-tetramethylaniline hydrochloride, such as 2,5-(N,N-dimethyl)aniline hydrochloride dimethylene bis-(tetramethylene sulfonium chloride) with alkali metal hydroxide to form a cycloalkylene sulfonium salt precursor polymer, and then heating the precursor polymer under conditions to produce the amino substituted phenylene vinylene polymer, such as poly(2-(N,N-dimethylamino) phenylene vinylene).
Type:
Grant
Filed:
May 10, 1995
Date of Patent:
December 24, 1996
Assignee:
The United States of America as represented by the Secretary of the Navy
Inventors:
John D. Stenger-Smith, William P. Norris, Andrew P. Chafin
Abstract: Novel polythiophene compounds useful as anti-tumor agents are described. Preferred compounds of the formula: ##STR1## wherein n is 0-2 and R.sub.2 and R.sub.3 are optionally substituted 2-thienyl or 3-thienyl have been found to exhibit selective cytotoxic activity against transformed human cells. Pharmaceutical compositions containing the described polythiophene compounds are expected to exhibit good chemotherapeutic activity against slow growing tumors based on tumor cell line assays. A method for treating patients having tumors utilizing the disclosed polythiophene compounds is also described.
Type:
Grant
Filed:
April 8, 1994
Date of Patent:
November 26, 1996
Assignees:
Purdue Research Foundation, International Technology Research Institute
Inventors:
Ching T. Chang, Ching-Jer Chang, Chen-Tao Lee, Fen-Lan Lin, Jih-Dar Tsai, Curtis L. Ashendel, Thomas C. K. Chan, Robert L. Geahlen, David J. Waters
Abstract: The present invention provides compounds having 12-lipoxygenase inhibitory effect and medicines inhibiting 12-lipoxygenase selectively, and relates to novel coumarin derivatives and medicines containing the compounds as effective ingredients. Furthermore, this invention relates to compounds capable of converting to compounds inhibiting 12-lipoxygenase activities selectively according to the cleavage of modified moieties in vivo and medicines inhibiting 12-lipoxygenase selectively, and relates to novel coumarin derivatives having acyl groups as modified moieties and medicines containing the compounds as effective ingredients. The compounds of the present invention can inhibit 12-lipoxygenase strongly and selectively, and being useful as medicines for preventing and treating various circulatory diseases such as arteriosclerosis and vasospasm and for preventing of the metastasis of some kinds of cancers, and show low toxicity and few side effects.
Abstract: This invention is concerned with an improved process for the synthesis of and intermediate en route to 5,6-dihydro-(s)-4-(ethylamino)-(s)-6-methyl-4h-thieno[2,3-b]thiopyran-2-su lfonamide 7,7-dioxide and related compounds. The instant process reduces the reaction time for the synthesis of the key intermediate from 3 to 4 days to from about 2 to about 4 hours while retaining the high enantiomeric purity of the product.
Type:
Grant
Filed:
April 26, 1995
Date of Patent:
November 12, 1996
Assignee:
Merck & Co., Inc.
Inventors:
David J. Mathre, Paul Sohar, Lynn M. Brown
Abstract: Disclosed are compounds of Formula I: ##STR1## or a pharmaceutically acceptable salt or solvate thereof, wherein: R.sup.4 is alkenyl, alkoxy, or --OH.Also disclosed are pharmaceutical compositions containing compounds of Formula I, methods for inhibiting tumor necrosis factor-.alpha., and methods for treating septic shock, inflammation, or allergic disease.
Type:
Grant
Filed:
December 6, 1993
Date of Patent:
November 12, 1996
Assignee:
Schering Corporation
Inventors:
Pauline C. Ting, Richard J. Friary, Wing C. Tom, Joe F. Lee, Vera A. Seidl
Abstract: A pharmaceutical composition containing alpha-lipoic acid, dihydrolipoic acid, metabolites of alpha-lipoic acid (inter alia bisnortetralipoic acid and tetranorlipoic acid), optical isomers R- and S- forms of alpha-lipoic acid in oxidized and reduced form together with a vitamin, especially vitamins A, B1, B2, B6, B12, C and E and their pharmaceutically acceptable salts. The compositions are useful for producing analgesic, anti-inflammatory, antidiabetic, cytoprotective, anti-ulcer, antinecrotic, neuroprotective, detoxifying, anti-ischemic, liver function regulating, anti-allergic, immune-stimulating and antioncogenic effects.
Type:
Grant
Filed:
March 14, 1995
Date of Patent:
October 29, 1996
Assignee:
Asta Medica Aktiengesellschaft
Inventors:
Carl-Heinrich Weischer, Heinz Ulrich, Klaus Wessel
Abstract: New antineoplastic substances have been isolated, structurally elucidated and synthesized having a general structural formula of: ##STR1## wherein: R.sub.1 is OH or OCH.sub.3 ;R.sub.2 is H or OCH.sub.3 ; or R.sub.1 R.sub.2 is --OCH.sub.2 O--;R.sub.3 is H or OH; andR.sub.4 is OH or OCH.sub.3.These substances have been denominated "combretastatin A-1, -A-2, -A-3, -B-1, -B-2, -B-3 and -B-4". preparation containing the substances and methods of treating a host inflicted with a neoplastic growth with the preparation is described.
Type:
Grant
Filed:
November 15, 1994
Date of Patent:
October 29, 1996
Assignee:
Arizona Board of Regents acting on behalf of Arizona State University
Abstract: The present invention provides compounds with nitrogen-containing non-basic side chains of formula II ##STR1## wherein R.sup.1 and R.sup.2, independently, are H, OH, O(C.sub.1 -C.sub.6 alkyl), O--C(O)--(C.sub.1 -C.sub.6 alkyl), O--C(O)--O(C.sub.1 -C.sub.6 alkyl), O--C(O)--Ar, O--C(O)--O--Ar, O--SO.sub.2 --(C.sub.4 -C.sub.6 alkyl), chloro, fluoro, or bromo;W is CHOH, C(O), or CH.sub.2 ;Y is (CH.sub.2).sub.n, or CH(C.sub.1 -C.sub.4 alkyl);V is S, 0, or CH.sub.2 CH.sub.2 ;n is 1, 2, or 3; andAr is optionally substituted phenyl.The present invention also provides pharmaceutical compositions containing compounds of formula II, optionally containing estrogen or progestin, and the use of such compounds, alone, or in combination with estrogen or progestin, for alleviating the symptoms of post-menopausal symptoms, particularly osteoporosis, cardiovascular related pathological conditions, and estrogen-dependent cancer.
Abstract: A stable lyophilized composition of the antitumor alkylating agent thiotepa and a method of preparing such a composition via co-lyophilization of the active ingredient with a pharmaceutical acceptable alkalizing agent.
Type:
Grant
Filed:
August 2, 1994
Date of Patent:
October 1, 1996
Assignee:
American Cyanamid Company
Inventors:
Mannching S. Ku, Jorge Velez, Rodney J. Hoffman, Lourdes Zamora
Abstract: Inter alia, an iodophor preparation composition comprising, in addition to a carrier, an iodide source, an oxidant and an acid source, characterised in that at least one of the iodide source, the oxidant and the acid source is only available for reaction with the other components when dissolved in an aqueous medium at the point-of-use is disclosed.
Abstract: There is described a low-foaming, nonsilicone, aqueous textile auxiliary composition comprising(a) a homopolymer of an ethylenically unsaturated sulfonic or carboxylic acid or an anhydride thereof,(b) a nonionic surfactant of formula ##STR1## wherein R is an aliphatic radical of at least 8 carbon atoms,R.sub.1 is hydrogen, C.sub.1 -C.sub.8 alkyl, a cycloaliphatic radical of at least 5 carbon atoms, styryl, an unsubstituted or halogen substituted C.sub.1 -C.sub.10 alkylisocyanato or an unsubstituted or by a hetero atom substituted cycloalkylisocyanato or cycloalkenylisocyanato radical,"alkylene" denotes an alkylene radical of 2 to 4 carbon atoms, andp is an integer from 2 to 60, and optionally(c) a hydrotropic agent.The textile auxiliary composition is suitable for use as dispersants and for wetting, washing and/or bleaching fiber materials.
Type:
Grant
Filed:
June 7, 1995
Date of Patent:
September 24, 1996
Assignee:
Ciba-Geigy Corporation
Inventors:
Christian Guth, Albert Stehlin, Christoph Krohnke
Abstract: The use of nicotinic anilide derivatives of the general formula ##STR1## where the substituents have the following meanings: R.sup.1 halogen, methyl, trifluoromethyl, methoxy, methylthio, methylsulfinyl, methylsulfonylR.sup.2 unsubstituted or halogen-substituted alkyl, unsubstituted or halogen-substituted alkenyl, alkynyl, unsubstituted or halogen-substituted alkoxy, unsubstituted or halogen-substituted alkenyloxy, alkynyloxy, cycloalkyl, cycloalkenyl, cycloalkyloxy, cycloalkenyloxyfor combating Botrytis, and nicotinic anilides of the formula I.
Type:
Grant
Filed:
June 7, 1995
Date of Patent:
September 17, 1996
Assignee:
BASF Aktiengesellschaft
Inventors:
Karl Eicken, Norbert Goetz, Albrecht Harreus, Eberhard Ammermann, Gisela Lorenz, Harald Rang
Abstract: This invention provides substituted benzimidazoles which are useful in treating or preventing conditions associated with .beta.-amyloid peptide. Some such conditions associated with .beta.-amyloid peptide include Alzheimer's Disease, Down's Syndrome and amyloidosis of the Dutch type.
Type:
Grant
Filed:
April 29, 1994
Date of Patent:
September 3, 1996
Assignee:
Eli Lilly and Company
Inventors:
William H. W. Lunn, James A. Monn, Dennis M. Zimmerman
Abstract: Detergent compositions are formed into tablets for dispensing. These tablets can be retained in a flexible plastic bag having a rigid opening and tapered midsection. The rigidity of the tablets enables the bag to retain its shape and prevent hydratable detergents from clogging up the dispenser. A preferred detergent formulation is a high-caustic detergent composition which includes a combination of sodium tripolyphosphate and sodium tripolyphosphate hexahydrate, defoaming surfactant, polycarboxylate and a processing and dissolution aid such as propylene glycol. This detergent composition, when tableted, provides an extremely uniform dissolution rate minimizing any temperature peaks that can occur in dispensing high-caustic detergent.
Abstract: Bicyclic sulfones of the formula I ##STR1## in which Y is a halogen atom,Z is a halogen atom or hydrogen,m and n, that are different and represent an integer 0 or 1,A and B each represent hydrogen or together represent a valency bond,X.sub.1 and X.sub.2 each represent NR.sub.1 R.sub.2 or, if A and B represent a valency bond, one of the two residues X.sub.1 or X.sub.2 represents hydrogen and the other represents NR.sub.1 R.sub.2,R.sub.1 denotes a C.sub.1 -C.sub.6 alkyl, C.sub.3 -C.sub.7 cycloalkyl, C.sub.2 -C.sub.6 alkenyl or a benzyl residue substituted if desired, by halogen, C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.6 alkoxy or hydroxy andR.sub.2 denotes hydrogen or a residue from the definition of R.sub.1 orR.sub.1 and R.sub.2 together with the nitrogen atom form a heterocyclic ring which if desired, contains further heteroatoms and/or can be substituted by C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.6 alkoxy, C.sub.1 -C.sub.
Abstract: The invention relates to 7-[5-hydroxy-2-(hydroxyhydrocarbyl or heteroatom-substituted hydroxy hydrocarbyl)-3-hydroxycyclopentyl(enyl)] heptanoic or heptenoic acids and derivatives of said acids, wherein one or more of said hydroxy groups are replaced by an ether group. The compounds of the present invention are potent ocular hypotensives, and are particularly suitable for the management of glaucoma.
Abstract: The invention pertains to use of phthaloylhydrazide derivatives and salts thereof as anti-inflammatory and antitoxic agents in human and veterinary medicine, and it pertains in particular to use of 5-aminophthaloylhydrazide and of the sodium salt thereof.