Abstract: Compounds of formula (I) or pesticidally acceptable salts thereof, compositions containing them and methods of use.

Abstract: The present invention relates to therapeutic associations for the treatment of cancer, comprising an effective amount of a camptothecin, or a camptothecin derivative, with an effective amount of an alkylating agent, such as melphalan, dacarbazine, or cyclophosphamide, and methods of using such therapeutic associations.

Abstract: The present invention provides a novel thermosensitive cyclotriphosphazene-platinum complex conjugates represented by Formula 1, wherein m is a repeating unit of poly(alkoxyethylene glycol) selected from the integers 2, 7 and 12; n represents the length of the alkyl chain selected from the integers 0, 1, 2 and 3; x represents the length of the anionic amino acid residue selected from the integers 0 (amino malonic acid derivatives), 1 (aspartic acid derivatives) and 2 (glutamic acid derivatives); A2 is a bidentate chelating diamine selected from the group consisting of 2,2-dimethyl-1,3-propanediamine (dmpda), trans(±)-1,2-diaminocyclohexane (dach) and 1,1-diaminomethylcyclohexane (dmach).

Abstract: A method for inhibiting the growth of tumors and cancers in mammals comprising administering a chemotherapeutic agent to significantly reduce the tumor in mass and then administering a benzimidazole derivative. Potentiators can also be included in the benzimidazole composition.

Abstract: A method for inhibiting the growth of tumors and cancers in mammals comprising administering a chemotherapeutic agent to significantly reduce the tumor in mass and then administering a benzimidazole derivative. Potentiators can also be included in the benzimidazole composition.

Abstract: The present invention relates to the field of cancer, and in particular hormone dependent cancers including, but not limited to prostate, breast, endometrial, ovarian, thyroid, bone, and testis. The present invention also relates to the use of steroid analogues, and in particular analogues of &Dgr;5-androstene-3-&bgr;, 17&agr;-diol, and its epimer &Dgr;5-androstene-3-&bgr;, 17&bgr;-diol for the treatment and prevention of cancer.

Abstract: A method for treating a tumor includes a first treatment procedure using a conventional cancer treatment technique, and a second treatment procedure which includes administering an effective amount of squalamine. Synergistically effective amounts are preferred. The first treatment procedure may be a treatment with one or more conventional cytotoxic chemical compounds. As examples, the cytotoxic chemical compound may be a nitrosourea (such as BCNU), cyclophosphamide, doxorubicin, 5-fluorouracil, paclitaxel and its derivatives, cisplatin or other platinum containing cancer treating agents. Alternatively, the first treatment may be a treatment with one or more conventional anti-hormonal agents. As examples, the anti-hormonal agents may be a LHRH (luteinizing hormone releasing hormone) agonist or an anti-androgen such as flutamide, biclutamide, nilutamide, and luprolide. These conventional cancer treatments compounds and the squalamine may be administered by any suitable route.

Abstract: The invention relates to methods and products for inducing an immune response using immunostimulatory nucleic acids. In particular the immunostimulatory nucleic acids preferentially induce a Th2 immune response. The invention is useful for treating and preventing disorders associated with a Th1 immune response or for creating a Th2 environment for treating disorders that are sensitive to Th2 immune responses.

Abstract: The present invention provides methods for treating mammalian cancer tumors, preferably solid tumors, comprising administering to a mammal in need of such treatment an effective amount of a 1,2,4-benzotriazine oxide as defined in Formula I or pharmacologically acceptable salts of said compound; and administering to the mammal from about one half hour to about twenty-four hours after administering the 1,2,4-benzotriazine oxide an effective amount of a chemotherapy agent to which the tumor is susceptible. The invention also provides kits for treatment of such tumors which comprise a chemotherapy agent and a cytotoxicity-enhancing amount of a 1,2,4-benzotriazine oxide as defined in Formula I.

Abstract: A method for inhibiting the growth of tumors and cancers in mammals comprising administering a chemotherapeutic agent to significantly reduce the tumor in mass and then administering a benzimidazole derivative. Potentiators can also be included in the benzimidazole composition.

Abstract: This invention is to provide a pharmaceutical composition for antagonizing CCR5 which comprises a compound of the formula: wherein R1 is an optionally substituted 5- to 6-membered ring; W is a divalent group of the formula: wherein the ring A is an optionally substituted 5- to 6-membered aromatic ring, X is an optionally substituted C, N or O atom, and the ring B is an optionally substituted 5- to 7-membered ring; Z is a chemical bond or a divalent group; R2 is (1) an optionally substituted amino group in which a nitrogen atom may form a quaternary ammonium, etc., or a salt thereof.

Abstract: The present invention provides immunogenic compositions and methods for inducing enhanced immune responses using an antigen and a combination of water soluble polymer and an amphiphilic compound.

Abstract: Disclosed are catalyst compositions comprising one or more transition metals selected from the Group VIII metals and rhenium and one or more chlorophosphite compounds having the general Formula wherein R1 and R2 are aromatic hydrocarbyl radicals. Also disclosed are catalyst solutions comprising one or more the above chlorophosphite compounds, rhodium and a hydroformylation solvent, and hydroformylation processes wherein olefins are contacted with carbon monoxide, hydrogen and the catalyst solution to produce aldehydes.

Abstract: Inositol derivatives, compositions comprising inositol derivatives, and methods for using compositions comprising inositol derivatives as agents for inhibiting superoxide anion production are described. The inositol derivatives are obtainable via conventional organic synthesis. The inositol derivatives inhibit superoxide anion produced by neutrophils and macrophages which cause tissue damage.

Abstract: A soluble polyphosphazene polyelectrolyte immunoadjuvant is disclosed. In one embodiment, the polymeric adjuvant is poly[di(carboxylatrophenoxy)phosphazene] which is in the form of a microsphere and which is adsorbed with antigen after formation of the microsphere. The immunoadjuvant can be administered intranasally.

Abstract: An amorphous solid dispersion of efonidipine hydrochloride having a high intestinal absorbability can be formed by subjecting a mixture containing efonidipine hydrochloride of the formula (I), hydroxypropylmethylcellulose acetate succinate and optionally a thermostabilizer to a step A of heat treatment at from 85 to 140° C. or mechanochemical treatment at from 0 to 140° C., and then to a step B of dipping treatment into a water-containing solution, impregnation treatment with a water-containing solution or contacting treatment with a water vapor-containing gas; or treating the above-mentioned mixture with a hot steam at from 100 to 140° C. and a high pressure. Further, in the above-mentioned step A, the mixture is subjected to high frequency heating, making it possible to give a solid dispersion of efonidipine hydrochloride having a high intestinal absorbability without using the step B. This process is quite advantageous in the production in that the use of an organic solvent is not required.

Abstract: The invention relates to the use of G-CSF in combination with a chemotherapeutic agent (in particular, cyclophosphamide) to produce a pharmaceutical preparation for boosting the mobilization of hematopoietic stem cells from bone marrow in the treatment of diseases requiring peripheral stem cell transplantation. The claimed combination results in more efficient leukapheresis, e.g. before myeloblative or myelotoxic therapy.

Abstract: A method for treating a tumor includes a first treatment procedure using a conventional cancer treatment technique, and a second treatment procedure which includes administering an effective amount of squalamine. The first treatment procedure may be a treatment with one or more conventional cytotoxic chemical compounds. As examples, the cytotoxic chemical compound may be a nitrosourea (such as BCNU), cyclophosphamide, adriamycin, 5-fluorouracil, paclitaxel and its derivatives, cisplatin or other platinum containing cancer treating agents. The cytotoxic chemical compound and the squalamine may be administered by any suitable route. The first treatment procedure may take place prior to the second treatment procedure, after the second treatment procedure, or the two treatment procedures may take place simultaneously. In one example, the first treatment procedure (e.g., a one time intravenous dosage of BCNU) is completed before the second treatment procedure with squalamine begins.

Abstract: The present invention provides a method of killing a cell by first administering to the cell a vitamin D derivative and subsequently administering to the cell a cytotoxic agent. Where the cell is within a tumor, the present invention provides a method of retarding the growth of the tumor by first administering the vitamin D derivative to the tumor and subsequently administering to the tumor the cytotoxic agent.

Abstract: (R)-Ifosfamide is administered as a cytotoxic drug, in order to minimize side effects. (S)-Ifosfamide may be administered subsequently.

Abstract: A polyphosphazene polyelectrolyte immunoadjuvant having improved water solubility, a vaccine composition of the immunoadjuvant and an antigen or immunogen and methods of their use in producing or enhancing an immunoprotective response in a host are disclosed.

Abstract: This invention provides for pharmaceutical formulations of compounds which are useful as protective agents when administered to patients also receiving antineoplastic drugs. The invention also includes methods of reducing the toxicity of various antineoplastic agents by administering an effective amount of the protective agent to a patient receiving one or more antineoplastic agents. The compounds useful as protective agents have either a sulfhydryl moiety or are reducible disulfides.

Abstract: The present patent application discloses compounds having the formula ##STR1## or a pharmaceutically acceptable salt thereof wherein R.sup.1, X and R.sup.5 have the meanings set further in the specification.A is a ring of five to seven atoms fused with the benzo ring at the positions marked a and b.The compounds are useful in the treatment of cerebrovascular disorders for example.

Abstract: The present invention provides a purified retinoid compound characterized by a molecular mass of about 320 daltons and an atomic composition of C.sub.20 H.sub.32 O.sub.3. The present invention also provides a purified retinoid compound having the following structure: ##STR1## wherein the configuration of C7, C9, and C11 double bond independently is Z or E and the absolute configuration at C13 and C14 is independently R or S; wherein R1 is hydroxyl, alkyl, alkyl halide, alcohol, ester, ether, aldehyde, ketone, carboxylic acid, carboxylic ester, acyl halide, amide, nitrile, or amine; wherein R2 and R3 are independently hydroxyl, halide, alkoxy, ester, alkyl, alcohol, ether, aldehyde, ketone, carboxylic acid, carboxylic ester, nitrile, amine, azide, alkyl halide, acid halide, acid azide, or amide; or wherein R2 and R3, or R1 and R2 are replaced by a 13,14-oxirane or a 14,15-oxirane group, respectively.

Abstract: A polyphosphazene polyelectrolyte immunoadjuvant having improved water solubility, a vaccine composition of the immunoadjuvant and an antigen or immunogen and methods of their use in producing or enhancing an immunoprotective response in a host are disclosed.

Abstract: The encephalopathy caused by ifosfamide and similarly acting compounds can be prevented or treated by the administration of methylene blue or another compound which is able to oxidize a reduced flavin moiety. Pyritinol is able to reduce other aspects of ifosfamide toxicity.

Abstract: Disclosed are catalyst systems comprising one or more transition metals selected from the Group VIII metals and rhenium and one or more fluorophosphite compounds having the general formula ##STR1## wherein R.sup.1 and R.sup.2 are hydrocarbyl radicals. Also disclosed are catalyst solutions comprising one or more the above fluorophosphite compounds, rhodium and a hydroformylation solvent, and hydroformylation processes wherein olefins are contacted with carbon monoxide, hydrogen and the catalyst solution to produce aldehydes.

Abstract: The present invention is directed to compounds useful for the regulation of cholesterol of Formula I, methods for using them and pharmaceutical compositions thereof, ##STR1## wherein Ar and Ar.sup.1 are each independently selected from unsubstituted or substituted phenyl which substituents are from 1-5 in number and are each independently selected from alkyl, alkoxy, hydroxy, halogen, nitro, trifluoromethyl, COOH, and COOalkyl;X is --NH--, --O--, --S--, or --(CH.sub.2).sub.0-4 --, andR is hydrogen, alkyl, or phenyl.

Abstract: Compounds of formula (II) ##STR1## wherein R is a biphenyl group optionally substituted by one or more substituents, the same or different, selected among halogen atoms, hydroxy groups, alkoxy, alkyl or thioalkyl groups having from 1 to 6 carbon atoms in the alkyl moiety, carboxylic groups, nitro groups, amino, mono- or di-alkylamino groups having from 1 to 6 carbon atoms in the alkyl moiety; R.sub.1 is a hydrogen atom or a straight or branched C.sub.1 -C.sub.4 allyl; R.sub.2 is a straight or branched C.sub.1 -C.sub.6 alkyl or an arylalkyl having from 1 to 6 carbon atoms in the alkyl moiety wherein the aryl is a phenyl, a naphthyl or a 5 or 6 membered aromatic heterocycle with one or two heteroatoms selected among nitrogen, oxygen and sulphur, optionally substituted as above indicated for the R substituent; R.sub.3 is a straight or branched C.sub.1 -C.sub.

Abstract: The invention relates to improved ifosfamide preparations which are distinguished in that as primary auxiliary a polysaccharide, in general a glycan, preferably dextran, starches or cellulose, in particular dextrans having an MW of 20,000 to 85,000, modified starches such as hydroxyethyl starch and chemically modified celluloses such as hydroxyethylcellulose and sodium carboxymethylcellulose, a glycol ether, preferably polyethylene glycol, in particular polyethylene glycols having a molecular weight of 600 to 6000 or an amino acid, preferably alanine, leucine or glutamic acid, is added to them.The improved ifosfamide preparation can also contain as an auxiliary a pharmaceutically customary buffer, for example acetate, citrate or tris buffer, preferably phosphate buffer.In addition, improved ifosfamide preparations are obtained by addition of NaHCO.sub.3.The ifosfamide preparations according to the invention can comprise one or a combination of several auxiliaries.

Abstract: A compound of formula (I): ##STR1## or a pharmaceutically acceptable salt, or solvate thereof, wherein,R.sup.o represents an aryl group, optionally substituted;X represents O or S;R.sup.1 and R.sup.1a each independently represents hydrogen or an alkyl group;R.sup.2 represents OCH.sub.2 CO.sub.2 H, or an ester or amide thereof, or R.sup.2 represents a moiety of formula (b): ##STR2## wherein R.sup.4 represent hydrogen, alkyl, hydroxyalkyl, arylalkyl, aralkyloxyalkyl or cycloalkyl and R.sup.5 represent hydroxy, alkoxy, arylalkyloxy, hydroxyalkyloxy, alkoxyalkyloxy, arylalkoxyalkyloxy, cycloalkyloxy, hydrogen, alkyl, substituted alkyl, cycloalkyl, aryl, arylalkyl, arylalkyloxyalkyl or R.sup.5 together with OR.sup.4 represents O(CH.sub.2).sub.n O wherein n is 2, 3 or 4; andR.sup.3 represents hydrogen, halogen, alkyl or alkoxy or R.sup.3 together with R.sup.

Abstract: An insecticide composition is enhanced from the standpoint of its ability to be absorbed by insects, such as red fire ants, particularly dithiophosphate ester pesticides by the addition of a small amount of a water soluble non-aromatic polyorganic acid or salt form thereof such as polyaspartic acid, particularly preferred with a molecular weight in the range of about 3000 to 40,000.

Abstract: Compounds of the formula I, ##STR1## in which the symbols or substituents A, B, D, D*, E and E* have the meanings given in the specification, inhibit aspartyl proteases and are suitable for controlling viral diseases.

Abstract: An insecticide composition is enhanced from the standpoint of its ability to be absorbed by insects, such as red fire ants, particularly dithiophosphate ester pesticides by the addition of a small amount of a water soluble non-aromatic polyorganic acid or salt form thereof such as polyaspartic acid, particularly preferred with a molecular weight in the range of about 3000 to 40,000.

Abstract: The present invention is directed to novel phosphorous-containing inhibitors of cysteine or serine proteases. Methods for the use of the protease inhibitors are also described.

Abstract: The subject invention involves a method for treating hyperproliferative conditions in mammalian epithelial cells comprising administering to the mammal a composition containing a safe and effective amount of a lysophosphatidic acid compound or derivative having the structure ##STR1## or a cyclic derivative thereof having the structure ##STR2## or a pharmaceutically acceptable salt thereof, wherein: a) --Y-- is --0-- or --CH.sub.2 --;b) --Z is --XH, --H or halo;c) each --X-- is independently --0-- or --S--; andd) --R is unsubstituted or substituted, saturated or unsaturated, straight or branched chain alkyl having from 11 to about 23 carbon atoms.

Abstract: A novel pharmaceutical composition having anti-bacterial and antiviral activity and method of treating diseases caused by bacterial and viral pathogens through stimulation of the immunologic system. The composition comprises selected amounts of chlorambucil, procarbazine and cyclophosphamide. Melphalan and liothyronine are primary options. Calcium may also be included as a desirable supplement. The method includes administering these components to a patient in an ordered, time-released manner.

Abstract: The subject invention relates to methods for regulating wrinkles in mammalian skin comprising topical application of a lysophosphatidic acid compound having the structure: ##STR1## or a cyclic derivative thereof having the structure: ##STR2## or a pharmaceutically acceptable salt thereof, wherein --R is unsubstituted or substituted, saturated or unsaturated, straight or branched chain alkyl having from 12 to about 23 carbon atoms; each --X-- is independently --O-- or --S--; and --Y-- is --O-- or --CH.sub.2 --.

Abstract: A method is provided for reducing side effects caused by chemotherapeutic agents by administering to a patient in need thereof a therapeutically effective amount of a composition including L-2-oxothiazolidine-4-carboxylate specifically for reducing hemorrhagic cystitis in a patient at risk of same.

Abstract: A process for preparing a pharmaceutical preparation consisting essentially of a lyophilized cake of cyclophosphamide monohydrate and a bulking agent which comprises freezing cyclophosphamide, a bulking agent, and water, lyophilizing part of the water, obtaining and melting a supersaturated cyclophosphamide-bulking agent solution, precipitating cyclophosphamide as a hydrated polymorph, refreezing the solution and lyophilizing the water not bound to cyclophosphamide or the bulking agent.

Abstract: A lyophilized pharmaceutical solid composition containing cyclophosphamide for reconstitution with water to provide a solution for oral or parenteral administration. This lyophilized cyclophosphamide solid composition demonstrates improved stability, solubility characteristics and enhanced appearance compared with currently available dry powder pre-mix compositions of cyclophosphamide. The lyophilized solid composition contains about 20 parts by weight of cyclophosphamide, about 11/4-2 parts by weight of water and from about 10-85 parts by weight of excipient which is comprised mainly of mannitol. Processes for making the composition are disclosed.

Abstract: A method of treating human tumors is provided in which tumors are regionally treated with a cytolytic, pre-activated, bifunctional alkylating agent, namely 4-hydroperoxycyclophosphamide. The treatment is effective against a variety of tumor types within the central nervous systems.

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: 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: Compounds of the present invention are those having the formula: ##STR1## where R.sub.1 and R.sub.3 are the same or different and are a linear or branched chain of 1 to 22 carbon atoms selected from the group consisting of alkyl, alkenyl or alkynyl or said C.sub.1 to C.sub.22 chains substituted with halo, --SR.sub.5, --OR.sub.5, --NHR.sub.5, --NR'.sub.5 R.sub.5 or --C(O)OR.sub.6 where R.sub.6 is hydrogen or C.sub.1 to C.sub.6 alkyl; R.sub.5 and R'.sub.5 are the same or different and are hydrogen, amino-alkyl substituted with phenyl, substituted phenyl, benzoyl, substituted benzoyl, heteroaryl or substituted heteroaryl; R.sub.2 is hydrogen, C.sub.1 to C.sub.6 alkyl, phenyl or substituted phenyl; R.sub.4 is hydrogen, C.sub.1 to C.sub.6 alkyl, phenyl or substituted phenyl; Z is sulfur or oxygen; m is an integer from 1 to 3; and n is an integer from 1 to 23.The compounds provide useful methods of inhibiting protein kinase C.

Abstract: A parmaceutical preparation consisting essentially of a lyophilized cake of cyclophosphamide monohydrate and lactose prepared by the process of freezing cyclophosphamide, lactose and water, lyophilizing part of the water, obtaining and melting a supersaturated cyclophosphamide-lactose solution, precipitating cyclophosphamide as a hydrated polymorph, refreezing the solution and lyophilizing the water not bound to cyclophosphamide or lactose.

Abstract: The invention discloses certain substituted .alpha.-aminoacids having the formula ##STR1## where m and n are 1 or 2, and R, R.sub.1, R.sub.2, R.sub.3 and Y have various significances, which compounds are useful in treating epilepsy, disorders associated with excess GH or LH secretion, anxiety, schizophrenia, depression, CNS degenerative disorders, cerebral hypoxic conditions and stress-related psychiatric disorders.

Abstract: A stable rapidly dissolving lyophilized composition of cyclophosphamide and an amino acid selected from the group consisting of glycine, valine and serine is provided which contains an amount of water which is equimolar to the amount of amino acid and the amount of cyclophosphamide in said composition; the composition is preferably prepared from a solution containing at least 2% (W/V) of the amino acid and having a pH in the range of 5.0 to 7.0.

Abstract: Ulcerative conditions of the gastro-intestinal tract, e.g., antiinflammatory-drug-induced ulcers, are treated or prevented by the administration of a potassium channel activator. Methods and combination products are also disclosed for the treatment of inflammatory conditions without causing ulceration of the gastrointestinal tract.