Abstract: A method of combatting cancer in a subject comprising administering to said subject dehydroepiandrosterone (DHEA) or an analog thereof in an amount effective to combat cancer is disclosed in which heart failure induced by the DHEA or analog thereof is combatted by administering to the subject a ubiquinone, in an amount effective to combat heart failure induced by the DHEA or analog thereof.A prefered DHEA analog for carrying out the invention is 16 alpha-fluoroepiandrosterone, and a preferred ubiquinone for carrying out the invention is Coenzyme Q.sub.10.
Abstract: A bisphosphonic acid derivative of the general formula (I): ##STR1## wherein A is an optionally substituted cyclic group; R.sup.1 is hydrogen atom or a lower alkanoyl group; R.sup.2, R.sup.3, R.sup.4 and R.sup.5 are the same or different and are hydrogen atom or a lower alkyl group; m is 0, 1 or 2; and n is an integer from 2 to 10, or a salt thereof is disclosed. A process for its production and a bone resorption inhibitor containing the compound of the general formula (I) or a salt thereof are also disclosed.
Abstract: This invention relates to bisphosphoryl hydrazine compounds and to compositions thereof which are useful as pesticides. The compounds of this invention are effective against soil insects, especially the corn rootworm.
Abstract: A method is provided for inhibiting cholesterol biosynthesis by inhibiting de novo squalene production employing methylene phosphonoalkylphosphinate compounds.
Abstract: Compounds of formula I ##STR1## wherein R, R.sub.1, R.sub.2 and q are as defined in the description, have valuable pharmacological properties and are especially effective as calcium metabolism regulators. They are prepared in a manner known per se.
Abstract: A method of enhancing the formation of bone tissue and/or eliminating late complications subsequent to bone surgery comprising administering an amount, which is safe and sufficient to promote the formation of bone tissue and/or eliminate late complications, of a compound of formula ##STR1## wherein X is H, OH, Cl, F or a methyl group and Y is Cl, OH, --(CH.sub.2).sub.2 --N(CH.sub.3)--(CH.sub.2).sub.4 --CH.sub.3, --(CH.sub.2).sub.n --CH.sub.3 or --(CH.sub.2).sub.n --NH.sub.2, wheren is zero or an integer of 1 to 8, --NHZ, where Z is pyridinyl or cycloheptyl, --SZ', where Z' is pyridinyl or chloro-substituted phenyl, or Y is a pyridinylsubstituted lower alkyl chain; or a non-toxic, pharmaceutically acceptable salt or ester thereof to a bone surgery patient.
Type:
Grant
Filed:
March 24, 1993
Date of Patent:
April 4, 1995
Assignee:
Leiras Oy
Inventors:
Risto T. Lehtinen, Markku Nyman, Pekka Paavolainen
Abstract: 3 and 4-substituted 2(5H)-furanone compounds influence the balance between bone production and bone resorption in mammals, including humans. The active compounds are administered to mammals, including humans, in an effective dose which ranges between 0.05 to 100 mg per kilogram, body weight, per day, for the purpose of influencing the balance between bone production and bone resorption, and particularly for treating osteoporosis.
Abstract: Methods for treating or preventing osteoporosis, including regimens for intermittent dosing of bone resorption inhibiting polyphosphonate compound or a pharmaceutically acceptable salt or ester of any such compound.
Abstract: Substituted aminoethane-1,1-bisphosphonic acids and aminoethane-1,1-alkylphosphinophosphonic acids, processes for their preparation and use thereofThe invention relates to compounds of the formula I ##STR1## in which R.sup.2, R.sup.3, R.sup.4 and R.sup.5 are a hydrogen atom or (C.sub.5 -C.sub.5)-alkyl, m is the integer 0 or 1, x is (C.sub.1 -C.sub.10)-alkyl, mono- or polysubstituted, a 5- or 6-membered ring having one nitrogen atom and optionally a further nitrogen or oxygen atom; aryl having 6 or 10 carbon atoms, which can be substituted; or cycloalkyl, to processes for the preparation of the compound of the formula I; to pharmaceuticals, and to their use for the treatment of osteoporosis and degenerative joint diseases.
Type:
Grant
Filed:
November 24, 1993
Date of Patent:
November 15, 1994
Assignee:
Hoechst Aktiengesellschaft
Inventors:
Hans Lang, Christoph Naumann, Ruth Raiss, Osamu Komiyama, Yoshiko Terui
Abstract: Novel acids, esters, and salts of phenyl, naphthyl, quinoxalinyl, and biphenyl bisphosphonic acids and 1,2-oxaphosphepins are described. These compounds are useful as antiinflammatory and anti-arthritic agents. Also described are known compounds of the phenyl, naphthyl, quinoxalinyl, and biphenyl bisphosphonate classes which are also useful as antiinflammatory and anti-arthritic agents. Representative compounds include [1,2-phenyldiyl]bis(methylene)bisphosphonic acid tetramethyl ester, [2,3-quinoxalindiyl]bis(methylene)bisphosphonic acid tetramethyl ester, [[3-(propyl)-4-(methoxy)-1,8-naphthalenediyl]bis(methylene)]bisphosphonic acid tetramethyl ester, [2,6-naphthalenediylbis(methylene)bisphosphonic acid tetraethyl ester, and [2,2'-biphenylenebis(methyl)]bisphosphonic acid tetramethyl ester. Representative oxaphosphepins include the preferred 3,4-dihydro-3-methoxy-7-(phenylmethoxy)-1H-naphth[1,8de][1,2]oxaphosphepin -3-oxide.
Abstract: Pharmaceutical compositions of bisphosphonic acids, and salts thereof, are prepared by direct compression/dry mix tablet formulation. These pharmaceutical compositions are useful in the treatment of disturbances involving calcium or phosphate metabolism, in particular, the treatment and prevention of diseases involving bone resorption, especially osteoporosis, Paget's disease, malignant hypercalcemia, and metastatic bone disease.
Type:
Grant
Filed:
December 2, 1992
Date of Patent:
October 25, 1994
Assignee:
Merck & Co., Inc.
Inventors:
Simon R. Bechard, Kenneth A. Kramer, Ashok V. Katdare
Abstract: A method is provided for treating a fungal infection which includes the step of administering a therapeutically effective amount of a phosphorus-containing squalene synthetase inhibitor.
Abstract: This invention relates to a method of lowering abnormally high serum cholesterol levels in the body without significantly reducing mevalonic metabolite synthesis and to novel pharmacological compositions containing as an active ingredient bisphosphonic acid and ester compounds containing a mono-, bi- or tricyclic ring linked with a bisphosphonate moiety through a basic amino alkylene group. This invention also provides novel bisphosphonate compounds and the processes for their preparation.
Type:
Grant
Filed:
May 1, 1992
Date of Patent:
May 31, 1994
Assignee:
Rhone-Poulenc Rorer Pharmaceuticals Inc.
Inventors:
John W. Ullrich, Raymond D. Youssefyeh, Daniel L. Cheney, Christopher J. Burns
Abstract: The present invention relates to compositions and methods which are effective against alveolar bone resorption and enhance the ability of a tooth moved in orthodontic therapy to remain in its new position or to stay in its original position when adjacent teeth are moved.
Abstract: Compositions and methods for protecting the luminal lining against gastric acid challenge are disclosed. The compositions provide effective anti-ulcer preparations which include phosphorylated alcohol. Phosphorylated alcohols comprise the active anti-ulcerogenic ingredient of the described therapeutic formulations. The preparation of unique linear and cyclic polyphosphorylated alcohols and methods of using same to protect the stomach luminal lining against acid challenge are also disclosed. Inositol hexaphosphate and mannitol hexaphosphate are demonstrated to provide therapeutic value in the treatment and prevention of gastro-erosive disease precipitated by exposure of biological tissues to highly acidic substances, for example, the gastric digestive acids. While inositol hexaphosphate alone at subthreshold concentrations provides a small gastro-protective activity, a combination of inositol hexaphosphate (at subthreshold concentrations) with polyvalent cations, such as Au.sup.+3 or Bi.sup.
Type:
Grant
Filed:
May 11, 1992
Date of Patent:
November 9, 1993
Assignee:
Board of Regents, The University of Texas System
Inventors:
Jose C. Barreto, Lenard M. Lichtenberger
Abstract: Platinum complexes of the general formula I[(R.sup.1 NH.sub.2).sub.n Pt].sub.q Y.sub.m X.sub.p (I)in which Y is a phosphonic acid ligand, and the preparation thereof, are described. The platinum complexes are suitable as active substances in pharmaceuticals, in particular for controlling cancers.
Abstract: Insecticided compositions comprising (a) a mixture of methylenedioxybenzene derivative compounds having in the benzene ring one, two and three substituents of the formula --CH.sub.2 O--(CH.sub.2 CH.sub.2 O).sub.2 --R.sub.1 wherein R.sub.1 is hydrogen or an alkyl group having from 1 to 4 carbon atoms and (b) an insecticide selected from the group consisting of synthetic pyrethroids, carbamates, organic phosphorates, avermentines and insect growth regulators.
Abstract: The invention relates to topically administrable pharmaceutical preparations containing pharmaceutically acceptable methanediphosphonic acid derivatives of formula ##STR1## and their salts, wherein R.sub.1 and R.sub.2 are hydrogen or C.sub.1 -C.sub.3 alkyl.
Type:
Grant
Filed:
December 20, 1991
Date of Patent:
August 18, 1992
Assignees:
Ciba-Geigy Corporation, Henkel Kommanditgesellschaft auf Aktien
Inventors:
Pier G. Ferrini, Carlo Voellmy, Peter H. Stahl, Jonathan Green
Abstract: The invention relates to topically adminstrable pharmaceutical preparations containing pharmaceutically acceptable methanediphosphonic acid derivatives of formula ##STR1## and their salts, wherein each of R.sub.1 and R.sub.2 is halogen, or wherein R.sub.1 is hydrogen and R.sub.2 is Ar--S-- or Het.sub.1 --NH--, in which Ar is unsubstituted or substituted phenyl and Het.sub.1 is unsubstituted or substituted, monocyclic, 5- or 6-membered monoaza-, diaza- or thiaza-aryl that is bonded via a ring carbon atom, or wherein R.sub.1 is hydrogen or hydroxy and R.sub.2 is --A--R.sub.3, in which A is alkylene and, on the one hand, R.sub.3 is Het.sub.2, which is Het.sub.1 bonded via a ring carbon or ring nitrogen atom, or, on the other hand, R.sub.3 is hydrogen, or amino that is unsubsituted or mono- or di-substituted by identical or different substituents selected from alkyl, cycloalkyl, Ar-alkyl, Ar-O-alkyl, Ar-S-alkyl and Het.sub.
Type:
Grant
Filed:
June 29, 1990
Date of Patent:
July 28, 1992
Assignee:
Ciba-Geigy Corporation
Inventors:
Pier G. Ferrini, Carlo Voellmy, Peter H. Stahl, Jonathan Green
Abstract: An acaricidal composition comprising as active ingredients(A) either .alpha.-cyano-3-phenoxybenzyl 2,2,3,3-tetramethylcyclopropanecarboxylate or .alpha.-cyano-3-phenoxybenzyl N-(2-chloro-.alpha.,.alpha.,.alpha.-trifluor o-p-tolyl)-valinate, and(B) O,O,O',O'-tetraethyl S,S'-methylene bis(phosphorodithioate), is very effectively applicable as a composition for controlling acarine pests such as two-spotted spider mite (Tetranychus urticae Koch), carmine spider mite (Tetranychus cinnabarinus Boisduval), Kanazawa spider mite (Tetranychus Kansawai Kishida), citrus red mite (Panonychus citri McGregor), European red mite (Panonychus ulmi Koch), broad mite (Polyphagotarsonemus latus Banks), etc. in areas cultivated with fruit trees, tea-plant, vegetables, flowering plants, etc.
Abstract: This invention relates to pyrindine-diphosphonic acid derivatives which are useful in treating or preventing diseases characterized by abnormal calcium and phosphate matabolism, in particular those which are characterized by abnormal bone metabolism. This invention further relates to pharmaceutical compositions which contain the novel compounds of the present invention, and to a method of treating or preventing diseases characterized by abnormal calcium and phosphate metabolism utilizing a compound of the present invention.
Type:
Grant
Filed:
July 3, 1990
Date of Patent:
April 14, 1992
Assignees:
The Procter & Gamble Company, The Procter & Gamble Company
Inventors:
James J. Benedict, Karen Y. Johnson, James J. Benedict, Karen Y. Johnson
Abstract: (Cycloalkylamino)methylenebis(phosphonic acid) represented by the general formula: ##STR1## in which, R, R.sup.1, R.sup.2, R.sup.3 and R.sup.4 represent a hydrogen atom or a lower alkyl group, and n represents an integer from 3 to 10, a lower alkyl ester thereof or a pharmaceutically acceptable salt thereof; and a bone-resorption inhibitor and an anti-arthritis containing the same.
Abstract: Pharmaceutical compositions and a method for inhibiting the growth of tumor cells by administering a tumor cell growth-inhibiting amount of a bis[bis (diphenylphosphino)hydrocarbon]-, bis[bis(diethylphsophino) hydrocarbon]-, bis[bis(diphenylphosphine-deithylphosphino) hydrocarbon]gold(I), silver(I) or copper(I) complex or a tris[bis(diphenylphosphino)ethane] dicopper(I) complex to an animal afflicted with said tumor cells.
Type:
Grant
Filed:
June 11, 1986
Date of Patent:
August 6, 1991
Assignee:
SmithKline Beckman Corporation
Inventors:
Susan J. Berners-Price, Randall K. Johnson, Christopher K. Mirabelli, Peter J. Sadler
Abstract: Compounds of the formula I ##STR1## in which R.sub.1 is an aromatic radical, n is 0, 1, 2 or 3, X is an oxy group, a thio group which can be oxidized or an imino group which is unsubstituted or has aliphatic substituents, alk.sub.1 and alk.sub.2 are identical or different divalent aliphatic radicals, and R.sub.2 is hydrogen or a monovalent aliphatic radical and salts thereof have properties which regulate calcium metabolism and can be employed for the treatment of diseases connected with disturbances in this metabolism. They are prepared, for example, by reacting a compound of the formula ##STR2## in which X.sub.3 is carboxyl with a phosphorylating agent and hydrolysing the primary product.
Abstract: Substituted aminomethylenebis(phosphonic acid) derivatives represented by the general formula: ##STR1## in which R.sup.1, R.sup.2, R.sup.3 and R.sup.4 may be the same or different, each represents a hydrogen atom or a lower alkyl group; "m" is zero or represents an integer from 1 to 4; and a ring "A" represents a cycloalkenyl group having 5 to 8 carbon atoms, a bicycloheptyl group, a bicycloheptenyl group or a saturated heterocyclic group having 4 to 7 carbon atoms and containing an oxygen atom, a sulfur atom, a sulfinyl group (--SO--) or a sulfonyl group (--SO.sub.2 --), or pharmaceutically acceptable salts thereof.
Abstract: Compounds of the general Formula (I) ##STR1## in which R is a hydrogen atom or a bromine atom, and R.sub.1 is a hydrogen atom, an SO.sub.2 OM group wherein M is a hydrogen or sodium atom, various sulphatide or phosphatide groups or a glucuronide group are disclosed for use in the prophylaxis and therapy of retroviral infections, especially infection by Human Immunodeficiency Virus. These compounds may be used concomitantly or in combination with various immunomodulators and/or antiviral agents.
Abstract: A method is provided for inhibiting tumor growth by administering to a subject an effective tumor-inhibiting amount of a compound selected from the group consisting of phytic acid, phytate salt, an isomer or hydrolysate of phytic acid or phytate salt, or a mixture of any combination thereof. The preferred method of administration is by oral dosages of about 2 to 4 grams/kilogram bodyweight per day.
Type:
Grant
Filed:
June 10, 1988
Date of Patent:
August 28, 1990
Assignees:
Linus Pauling Institute of Science & Medicine, Robert Sabin
Inventors:
Robert Sabin, Raxit Jariwalla, Stephen Lawson
Abstract: Remedies, preventives and functional diets for diabetic diseases, esp., diabetes, contain phytic acid or its salt or salts. The salt of phytic acid is a non-toxious metal salt, or a non-toxious salt with an organic base, a basic amino acid or an organic ester residue, and has a compositional form together with or separately from phytic acid.
Abstract: Novel cyclic geminal-diphosphonic acid compounds, and pharmaceutical compositions containing these compounds, which are useful for treating diseases characterized by abnormal calcium and phosphate metabolism; and a method of treating diseases characterized by abnormal calcium and phosphate metabolism utilizing these novel cyclic diphosphonic acid compounds.
Abstract: Compounds which are useful as inhibitors of cholesterol biosynthesis and thus as hypocholesterolemic agents are provided which have the structure ##STR1## Z is --(CH.sub.2).sub.n -- or --(CH.sub.2).sub.p --CH.dbd.CH--(CH.sub.2).sub.m --, wherein n is 1 to 5; p is 0, 1 or 2; m is 0, 1 or 2;R, R.sup.1 and R.sup.1a are the same or different and are H, lower alkyl or a metal ion; andR.sup.2 and R.sup.3 may be the same or different and are H or halogen.New intermediates used in preparing the above compounds and method for preparing same, pharmaceutical compositions containing such compounds and a method for using such compounds to inhibit cholesterol biosynthesis are also provided.
Abstract: A method is provided for treating Alzheimer's Disease by administering to a subject an effective symptom-alleviating amount of a compound selected from the group consisting of phytic acid, phytate salt, an isomer or hydrolysate of phytic acid or phytate salt, or a mixture of any combination thereof. The preferred method of administration is by oral dosages of about 1/2 to 3 grams/kilogram bodyweight per day.
Abstract: Disclosed are tetraalkyl enthenylidenebisphosphonates and a method for their manufacture. These compounds are suitable for use as antimicrobial agents in combating a number of pathogenic microorganisms, such as bacteria, yeasts, viruses, fungi and protozoa, when used together with a pharmaceutically-acceptable carrier. Also disclosed is a method for treating infectious diseases by administering a safe and effective amount of these tetraalkyl ethenylidenebisphosphonates.
Type:
Grant
Filed:
April 23, 1986
Date of Patent:
April 11, 1989
Assignee:
The Procter & Gamble Company
Inventors:
Charles R. Degenhardt, Duane L. Charbonneau
Abstract: Pharmaceutical compositions containing an effective, tumor cell growth-inhibiting amount of such a compound, and a method for treating tumor cells sensitive to such a di-gold phosphine compound which comprises administering a tumor cell growth-inhibiting amount of such a compound to an animal afflicted by said tumor cells.
Abstract: 2-Substituted-1,3-propylidenediphosphonates of formula (I), where A, R.sup.1 and R.sup.2 are defined in claim 1, are therapeutically active compounds, namely for the treatment of cardiovascular diseases.They can be prepared by reacting phosphonating agents with 1,3- dibromopropanes or ditosylates of 1,3-propanediols substituted in position 2. ##STR1## .
Type:
Grant
Filed:
July 16, 1985
Date of Patent:
September 29, 1987
Assignee:
Symphar S.A.
Inventors:
Craig L. Bentzen, Yves Guyon-Gellin, Kyriacos Kalathakis, Hieu T. Phan, Lan Nguyen Mong, Eric Niesor, Jean-Robert Rossier
Abstract: Novel cyclic geminal-diphosphonic acid compounds, and pharmaceutical compositions containing these compounds, which are useful for treating diseases characterized by abnormal calcium and phosphate metabolism; and a method of treating diseases characterized by abnormal calcium and phosphate metabolism utilizing these noval cyclic diphosphonic acid compounds.
Abstract: A method of improving the levels of formed blood elements in a patient having disease or therapy induced leukopenia comprising administering to said patient a therapeutically effective amount of a pharmaceutically acceptable, water or lipid soluble tertiary or quaternary amine having cholinergic or anticholinesterase activity.
Abstract: A granulor formulation of a mosquito larvicide is prepared by impregnating corncob granules with an oil suspension or solution of a suitable toxicant in order to deposit the material on the surface of the granules. The impregnated granules float and are suitable for dispersion over a wide variety of larval mosquito sources.
Abstract: Diphosphonic acid derivatives of Formula I ##STR1## wherein R is hydrogen, an alkali metal atom, an alkaline earth metal atom, or an alkyl group of 1-4 carbon atoms andA is derived from a carboxylic acid having anti-inflammatory and antiphlogistic activity and containing an aromatic or heteroaromatic group, of Formula IIACOOH (II),are pharmacologically efficacious compounds.
Type:
Grant
Filed:
January 27, 1983
Date of Patent:
March 5, 1985
Assignee:
Schering Aktiengesellschaft
Inventors:
Helmut Biere, Clemens Rufer, Irmgard Boettcher