Abstract: This invention provides a novel disubstituted 1,2,4-triazine compound or a pharmaceutically acceptable salt thereof, which has an aldosterone synthetase inhibitory activity and is useful for preventing and/or treating various diseases or conditions associated with aldosterone; a method for preparing it; use of it; as well as a pharmaceutical composition comprising it as an active ingredient. A compound of the general formula [I]: wherein RA is, for example, a group of the following formula (A-1): wherein ring A1 is, for example, a cycloalkyl group which may be substituted, and RB is, for example, a monocyclic cycloalkyl group, or a pharmaceutically acceptable salt thereof.

Abstract: The disclosure describes methods of synthesis of pyridazinone compounds as thyroid hormone analogs and their prodrugs. Preferred methods according to the disclosure allow for large-scale preparation of pyridazinone compounds having high purity. In some embodiments, preferred methods according to the disclosure also allow for the preparation of pyridazinone compounds in better yield than previously used methods for preparing such compounds. Also disclosed are morphic forms of a pyridazinone compound. Further disclosed is a method for treating resistance to thyroid hormone in a subject having at least one TR? mutation.

Abstract: Compounds and compositions useful for treating disorders related to KIT and PDFGR are described herein.

Abstract: The present invention generally concerns particular methods and compositions for antimicrobial therapy. In particular embodiments, the compositions target DXR. In some cases, the antimicrobial agent comprises an electron-deficient hydrophobic group that has interacts with Trp211 of DXR. In specific embodiments, the compound contains electron-deficient heterocyclic rings that specifically interact with the electron-rich indole ring of Trp211. In certain aspects, the compositions comprise a phosphate group, a pyridine group, and a hydroxymate group.

Abstract: This document discloses molecules having the following formula (Formula One) and processes related thereto.

Abstract: Disclosed is a compound which has a low molecular weight and has an activity of enhancing the production of EPO and/or an activity of enhancing the production of hemoglobin.

Abstract: The invention features compounds of the general formula: in which the variable groups are as defined herein, and to their preparation and use.

Abstract: The invention features compounds of the general formula: in which the variable groups are as defined herein, and to their preparation and use.

Abstract: The present invention provides a compound which is useful as an inhibitor against the kinase activity of EML4-ALK fusion proteins and mutant EGFR proteins. As a result of extensive and intensive studies on compounds having an inhibitory effect against the kinase activity of EML4-ALK fusion proteins and mutant EGFR proteins, the inventors of the present invention have found that the di(arylamino)aryl compound of the present invention has inhibitory activity against the kinase activity of EML4-ALK fusion proteins and mutant EGFR proteins. This finding led to the completion of the present invention.

Abstract: The invention features compounds of the general formula (I) in which the variable groups are as defined herein, and to their preparation and use.

Abstract: The present invention relates to a pesticide composition intended for protecting plants, crops or seeds against fungal diseases or insect damages, and the corresponding methods of protection by application of the said composition. More precisely, the subject of the present invention is a pesticide composition based on a tetrazolyloxime derivative and a fungicide or an insecticide active substance or compound.

Abstract: The present invention provides heterocyclic linker compounds useful for linking drug moieties to ligands. The compounds also include drug-ligand conjugates comprising a ligand capable of targeting a selected cell population, and a drug connected to the ligand by a heterocyclic linker moiety. The linker moiety comprises a peptide sequence that is a substrate for an intracellular enzyme, for example a cathepsin, that cleaves the peptide at an amide bond. The peptide further contains a self-immolating moiety which connects the drug and the protein peptide sequence. Upon cleavage of the peptide sequence by an intracellular enzyme the self-immolating moiety cleaves itself from the drug moiety such that the drug moiety is in an underivatized and active form.

Abstract: Active compound combinations are disclosed which comprise (A) a dithiino-tetracarboximide of formula (I) and a further insecticidally active compound (B). Methods for controlling animal pests such as insects and/or unwanted acarids and for curatively or preventively controlling the phytopathogenic fungi of plants or crops are also disclosed as well as the use of a composition according to the invention for the treatment of seed, to a method for protecting a seed and to the treated seed.

Abstract: The novel active compound combinations comprising compounds of the formulae (I) and (II) have very good insecticidal and acaricidal properties.

Abstract: Provided herein are compounds of the formula (I): as well as pharmaceutically acceptable salts thereof, wherein the substituents are as those disclosed in the specification. These compounds, and the pharmaceutical compositions containing them, are useful for the treatment of diseases such as obesity, hyperlipidemia, hypercholesterolemia and diabetes and other related disorders and diseases, and may be useful for other diseases such as NASH, atherosclerosis, cardiovascular diseases, hypothyroidism, thyroid cancer and other disorders and diseases related thereto.

Abstract: The present invention provides 5-azacytosine derivatives with antiviral activity, specifically having viral replication inhibiting properties, more particularly in DNA viruses such as pox-, papilloma- and herpes viruses in humans. The invention also provides pharmaceutical compositions comprising such 5-azacytosine derivatives as active ingredients in combination with pharmaceutically acceptable carriers, which are useful for the treatment of subjects suffering from viral infections.

Abstract: The invention relates to insecticidal mixtures for protecting plants against attack by pests comprising (a) compounds of the formula (I) ?in which W, X, Y, Z, A, B, D and G are each as defined in the disclosure, and (b) specified agonists or antagonists of nicotinic acetylcholine receptors.

Abstract: The invention relates to insecticidal mixtures for protecting plants against attack by pests comprising (a) compounds of the formula (I) ?in which W, X, Y, Z, A, B, D and G are each as defined in the disclosure, and (b) agonists or antagonists of nicotinic acetylcholine receptors.

Abstract: The invention relates to inhibitors of enzymes that bind to ATP or GTP and/or catalyze phosphoryl transfer, compositions comprising the inhibitors, and methods of using the inhibitors and inhibitor compositions. The inhibitors and compositions comprising them are useful for treating disease or disease symptoms. The invention also provides for methods of making phosphoryl transferase inhibitor compounds, methods of inhibiting phosphoryl transferase activity, and methods for treating disease or disease symptoms.

Abstract: The present invention relates to uses and methods for treating or preventing a viral infection selected from the group consisting of herpes simple virus, varicella zoster virus, respiratory syncytial virus and cytomegalovirus in a host comprising using a therapeutically effective amount of a compound having the formula I or a pharmaceutically acceptable salt thereof. The present invention also includes pharmaceutical compositions and combinations.

Abstract: Phenylalanine derivatives of formula (1) are described: in which: Ar1 is an aromatic or heteroaromatic group; L1 is a linker atom or group; R is a carboxylic acid or a derivative thereof; Ar2 is an optionally substituted aromatic or heteroaromatic group; and the salts, solvates, hydrates and N-oxides thereof. The compounds are able to inhibit the binding of &agr;4 integrins to their ligands and are of use in the prophylaxis and treatment of immune or inflammatory disorders.

Abstract: Resolved enantiomers of the formula (IA) and (IB) wherein B is a purine or pyrimidine base or aza and/or deaza analogs thereof are useful in antiviral pharmaceutical compositions to treat retroviral infections.

Abstract: The invention provides compounds of formula 1,

Abstract: The present invention relates to novel benzimidazole compounds that have useful antiviral activity. More specifically, the invention encompasses benzimidazole compounds that inhibit membrane fusion associated events such as viral transmission, reduce viral load or otherwise treat viral infections. The invention also encompasses the use of benzimidazole compounds as inhibitors of membrane fusion associated events, such as viral transmission. In another embodiment, the invention encompasses processes for making benzimidazole compounds, methods of using the benzimidazole compounds and compositions comprising the benzimidazole compounds. Finally, the invention provides methods for treating, preventing or ameliorating symptoms associated with respiratory infection, particularly that caused by Respiratory Syncytial Virus utilizing the novel benzimidazole compounds of the invention.

Abstract: This invention relates to compounds which are generally muscarinic M2/M3 receptor antagonists and which are represented by Formula I: 1

Abstract: N-Heterocyclic derivatives of the formula (I): 1

Abstract: The subject invention provides pharmaceutical compounds useful in the treatment of Type II diabetes. These compounds are advantageous because they are readily metabolized by the metabolic drug detoxification systems. Particularly, thiazolidinedione analogs that have been designed to include esters within the structure of the compounds are provided. This invention is also drawn to methods of treating disorders, such as diabetes, comprising the administration of therapeutically effective compositions comprising compounds that have been designed to be metabolized by serum or intracellular hydrolases and esterases. Pharmaceutical compositions of the ester-containing thiazolidinedione analogs are also taught.

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

Abstract: Compounds that inhibit DNA-dependent protein kinase, compositions comprising the compounds, methods to inhibit the DNA-PK biological activity, methods to sensitize cells the agents that cause DNA lesions, and methods to potentiate cancer treatment are disclosed.

Abstract: A method of using 1,2,4-benzotriazine oxides, some of which are novel compounds, as radiosensitizers and selective cytotoxic agents is disclosed. These compounds are shown to specifically radiosensitive hypoxic tumor cells. Some are additionally disclosed to be useful as specific cytotoxic agents for these cells. They also show an unexpected ability to radiosensitize aerobic cells following or preceding a hypoxic incubation of the cells with the drug. This provides a basis for selective radiosensitization of tumors compared to normal cells. A novel method for preparing the 1,2,4-benzotriazine oxides is also disclosed.

Abstract: A low volatile organic compound co-solvent system is disclosed for preparing emulsion concentrates of low melting organophosphorous insecticides wherein the bioefficacy of the insecticide active is significantly enhanced. The co-solvent system comprises a water-soluble ethoxylated fatty acid/rosin acid-nonionic surfactant composition.

Abstract: Compositions and methods for attracting, killing, and/or neutering populations of boll weevils and other insects which spend the winter in areas with thick vegetation are disclosed. With respect to boll weevils, certain plant compounds, when presented along with Grandlure, the synthetic pheromone of the cotton boll weevil (Anthonomus grandis Boh.), increase the capture of boll weevils by as much as 50% as compared to Grandlure alone. The compounds, beta-caryophyllene, eugenol and myrcene, are among those present in leaves in overwintering sites favored by boll weevils. With respect to controlling boll weevil populations, the compounds can be used alone, in combination with Grandlure, and/or in combination with compounds which are toxic to boll weevils or which inhibit their ability to develop normally or reproduce.

Abstract: Nucleotide phosphonate esters characterized by the presence of an ester linked group which is bonded to the phosphorus atom of phosphonate nucleotide analogs are disclosed. The analogs comprise an ester bond that is hydrolyzed in vivo to yield a corresponding phosphonate nucleotide analog. Methods and intermediates for their synthesis and use are described.

Abstract: Novel chemotherapeutic agents having utility in treating infectious diseases such as periodontal disease, certain urinary tract infections, and infectious urinary tract stones, are obtained by combining chemically a diphosphonate compound with a therapeutic agent effective against the foregoing diseases.

Abstract: An ophthalmically acceptable solution and a method useful for disinfecting and/or cleaning a contact lens. The solution comprises an oxidizing agent and a polyvinyl pyrrolidone having a molecular weight ranging from 10,000 to 100,000 daltons and reactive towards a chlorite oxidizing agent. The end groups of the polyvinyl pyrrolidone are preferably aldehydes. The oxidizing agent of this invention preferably is selected from the group comprising chlorine oxides. The solution preferably has a pH ranging from about 6 to about 8.5. The method of the invention comprises the steps of forming this solution and then contacting a contact lens with the solution.

Abstract: Novel indane and indene derivatives are described which are endothelin receptor antagonists.

Abstract: Novel indane and indene derivatives are described which are endothelin receptor antagonists.

Abstract: Novel indane and indene derivatives are described which are endothelin receptor antagonists.

Abstract: Compounds having the following formulae I and II, and pharmaceutically acceptable salts thereof, including dual inhibitors of ACE and NEP and selective ACE inhibitors: ##STR1## and wherein R, R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.5a, R.sup.5b, R.sup.6, R.sup.7, R.sup.11, q and r are defined herein.

Abstract: The present invention relates to novel heterocycle-substituted diphosphonic acids, and the pharmaceutically-acceptable salts and esters thereof, in which the diphosphonate-substituted carbon atom moiety is attached to a carbon atom in a nitrogen-containing six membered ring heterocycle, preferably a piperidine ring. The heterocycle-substituted diphosphonic acid compounds have the general structure: ##STR1## wherein Z is a nitrogen-containing six membered ring heterocycle moiety selected from piperidinyl, diazinyl and triazinyl; m, n and m+n are from 0 to 10; Q is a covalent bond or a moiety selected from oxygen, sulfur or nitrogen; and R.sup.1, R.sup.2, R.sup.3 and R.sup.4 are substituent groups.The present invention further relates to pharmaceutical compositions containing these novel compounds. Finally this invention relates to methods for treating or preventing diseases characterized by abnormal calcium and phosphate metabolism by utilizing a compound or pharmaceutical composition of the present invention.

Abstract: Substituted amides, agricultural compositions containing them and a method to control arthropods in agronomic and non-agronomic environments, the amides having formula (I) wherein X is oxygen or sulfur and Q, G and Y are as defined in the text.

Abstract: The invention provides a concentrate for dilution with water in the preparation of an agriculatural composition for application to crops, soil or animals and comprising an agricultural chemical whose agricultural activity varies with the pH of the water; and the invention provides a method of preparing such agricultural composition by mixing the concentrate with water and effecting such pH modification to the composition as is necessary to obtain a pH in the composition at which the agricultural activity of the chemical is acceptable. The concentrate comprises an active ingredient and a pH indicator for colouring the water, and the proportions of pH indicator and active ingredient are selected so that when the concentrate is diluted with water to provide an effective concentration of active ingredient in the water, the pH indicator indicates visually whether or not the pH of the water is suitable for acceptable agricultural activiy of the chemical.

Abstract: The present invention concerns new substituted sulfonamides, and the physiologically acceptable salts, complexes, esters and amides thereof, represented by the formula ##STR1## which is defined herein. Said compounds find application as anti-thrombotic and anti-asthmatic medicines.

Abstract: Compounds of the formula I ##STR1## in which R can be hydrogen or C.sub.1 -C.sub.4 -alkyl, R.sup.1 hydrogen, C.sub.1 -C.sub.6 -alkyl, aryl, aryl-C.sub.1 -C.sub.4 -alkyl, amino-C.sub.1 -C.sub.6 -alkyl, C.sub.1 -C.sub.6 -alkylamino-C.sub.1 -C.sub.4 -alkyl, C.sub.1 -C.sub.6 -dialkylamino-C.sub.1 -C.sub.4 -alkyl, C.sub.1 -C.sub.4 -alkoxy-C.sub.1 -C.sub.4 -alkyl, C.sub.1 -C.sub.4 -alkylthio-C.sub.1 -C.sub.4 -alkyl, C.sub.3 -C.sub.7 -alkenyl, R.sup.2 R.sup.1 or C.sub.2 -C.sub.7 -alkenyl, C.sub.1 -C.sub.6 -alkylmercapto, C.sub.1 -C.sub.6 -alkoxy, phenoxy-C.sub.1 -C.sub.4 -alkyl,amino, C.sub.1 -C.sub.4 -alkylamino, di-C.sub.1 -C.sub.4 -alkylamino, morpholino, thiomorpholino, pyrrolidino, piperidino, hexamethyleneimino, pyrasolino, imidazolino, n 0, 1 or 2 and R.sup.1 and R.sup.

Abstract: A compound of the formula: ##STR1## wherein A is a purin-9-yl group, a heterocyclic isostere of a purin-9-yl group, a pyrimidin-1-yl group or a heterocyclic isostere of a pyrimidin-1-yl group; E is hydrogen, --CH.sub.2 OH or --OH; and G and D are independently selected from hydrogen, C.sub.1 to C.sub.10 alkyl, --OH, --CH.sub.2 OH, --CH.sub.2 OR.sub.20 wherein R.sub.20 is C.sub.1 to C.sub.6 alkyl, --CH.sub.2 OC(O)R.sub.21 wherein R.sub.21 is C.sub.1 to C.sub.10 alkyl, --CH.sub.2 OC(O)CH(R.sub.22)(NHR.sub.23) wherein R.sub.22 is the side chain of any of the naturally occurring amino acids and R.sub.23 is hydrogen or --C(O)CH(R.sub.24)(NH.sub.2) wherein a R.sub.24 is the side chain of any of the naturally occurring amino acids, --CH.sub.2 SH, --CH.sub.2 Cl, --CH.sub.2 F, --CH.sub.2 Br, --CH.sub.2 I, --C(O)H, --CH.sub.2 CN, --CH.sub.2 N.sub.3, --CH.sub.2 NR.sub.1 R.sub.2, --CO.sub.2 R.sub.1, --CH.sub.2 CH.sub.2 OH, --CH.sub.2 CH.sub.2 OR.sub.20 wherein R.sub.20 is as defined above, --CH.sub.2 CH.sub.2 OC(O)R.sub.

Abstract: ULV plant protecting arthropodicidal formulation comprising alkyl aryl polyglycol ether as further additives in addition to the active ingredient(s) dissolved in the mixture of alphatic hydrocarbons and sunflower oil. The formulation according to the invention has an initial contact angle on the plant surface of >13.degree., after 20 minutes of >6.degree. and it is often 120 minutes still at least 2.degree..

Abstract: The invention is novel compounds of the formula: ##STR1## wherein: X is a phenyl or naphthyl ring optionally substituted in any position with one to four substituents of;(i) --R.sub.2, wherein R.sub.2 is C.sub.1 -C.sub.25 alkyl, C.sub.1 -C.sub.25 alkenyl, C.sub.1 -C.sub.25 alkoxy, C.sub.1 -C.sub.25 thioalkyl, C.sub.1 -C.sub.25 alkenyloxy, phenyl, phenoxy, substituted phenyl or substituted phenoxy wherein the substituents are C.sub.1 -C.sub.20 alkyl, C.sub.1 -C.sub.20 alkoxy, halogen and trifluoremethyl;(ii) hydrogen, halogen, trifluoromethyl, cyano and nitro;(iii) --CO.sub.2 R.sub.3, --CONHR.sub.3, --CHO, OCONHR.sub.3, and --NHCOR.sub.3 wherein R.sub.3 is C.sub.1 -C.sub.25 alkyl, C.sub.1 -C.sub.25 alkenyl, phenyl or substituted phenyl wherein the substituents are C.sub.1 -C.sub.20 alkyl, C.sub.1 -C.sub.20 alkoxy, halogen or trifluoromethyl;R.sub.1 is one to four substituents on the aromatic ring which may be in any position and are hydrogen, C.sub.1 -C.sub.5 alkyl, C.sub.1 -C.sub.5 alkoxy or halogen;--CH.sub.

Abstract: This invention relates to derivatives of propanoic acid of the formula ##STR1## Useful as fungicides, insecticides and miticides, to processes for preparing them, to compositions containing them, and to methods of using them to combat fungi, especially fungal infections of plants, and to kill or control insects and mites.

Abstract: Novel insecticides of the formula ##STR1## in which n is 0 or 1,X is S, O, ##STR2## Y is N or ##STR3## Z is a 5- or 6-membered nitrogen-containing heterocyclic ring, and R to R.sup.9 variously represent hydrogen or specified organic radicals.

Abstract: The present invention relates to the use of the sulphenic acid amides of the general formula (I) ##STR1## in which X represents identical or different halogen atoms,Y.sup.1 and Y.sup.2 are identical or different and represent hydrogen, halogen, alkyl, alkoxy, halogenoalkyl or NO.sub.2 andZ represents halogen, --OH, --NHOH or the group --OR.sup.1,in whichR.sup.1 denotes optionally substituted radicals from the series comprising alkyl, alkenyl, alkinyl, cycloalkyl, aryl, aralkyl and heterocyclyl, orZ represents the group ##STR2## in which R.sup.2 and R.sup.3 are identical or different and denote hydrogen or a heterocyclic radical, orZ represents the group --OMin which M denotes ammonium or the equivalent of an alkali metal, alkaline earth metal or heavy metal cation, for prolonging the duration of a high activity in agents for combating soil pests.