Abstract: A compound represented by the formula: [wherein R1 represents a hydrogen atom, a halogen, atom, alkyl group, etc., R2 represents a hydrogen atom, a halogen atom, alkyl group, etc., R3, R4, R5, R6 and R7 each independently represent a hydrogen atom, a halogen atom, a substitutable alkyl group, a substitutable alkenyl group, alkynyl group, a substituteable cycloalkyl group, etc., or R3, R4, R5, R6 and R7 may form a ring which may be substituted, which is formed by the adjacent two of them with carbon atoms to which the respective substituents are bonded, m and n each independently represent 0 or 1.] a salt thereof, an ester derivative thereof and an agricultural chemical containing the same as an effective ingredient, and a herbicidal composition containing the compound and a second herbicidally active compound as effective ingredients.

Abstract: The invention described herein relates to certain pyridazinedione N-substituted glycine derivatives of formula (I) which are antagonists of HIF prolyl hydroxylases and are useful for treating diseases benefiting from the inhibition of this enzyme, anemia being one example.

Abstract: Pharmaceutical compositions and methods of treatment are provided for treating amyloidosis, containing, as an active ingredient, at least one nitrogen-containing heteroaryl compound represented by the following general formula or a pharmacologically permitted salt thereof; together with nitrogen-containing heteroaryl derivatives, and pharmacologically permitted salts thereof: where, R1, R2, Z1-Z5, and A are as defined herein.

Abstract: Compounds complying with the general formula in which R either represents a halogen atom or a phenyl group substituted by one or more groups chosen from halogen atoms and (C1-C6)alkyl, (C1-C6)alkoxy, nitro, amino, trifluoromethyl, cyano, hydroxy, acetyl or methylenedioxy groups, or represents a pyridinyl group, a thienyl group, an indolyl group, or a pyrimidinyl group optionally substituted by one or more (C1-C6)alkoxy groups, where, of the two carbon-carbon bonds represented by , one is single and the other may be single or double. The compounds of this invention are useful as therapeutic agents.

Abstract: The present invention is directed to compounds having the structure wherein R1, R2, R3, R4, R5 and m are as defined herein. The compounds of this invention are novel therapeutic agents for the treatment of cancer, metabolic diseases and skin disorders in mammalian subjects. These compounds are also useful modulators of gene expression. They exert their activity by interfering with certain cellular signal transduction cascades. The compounds of the invention are thus also useful for regulating cell differentiation and cell cycle processes that are controlled or regulated by various hormones or cytokines. In particular, the invention relates to compounds that induce apoptosis of cancer cells and therefore may be used for the treatment or prevention of cancer, including advanced cancers and pre-cancerous cells.

Abstract: The present invention relates to a medicinal composition for preventing or treating pancreatic cancer, comprising 3-alkoxy-6-allylthiopyridazine or a pharmaceutically acceptable salt thereof as an effective ingredient. An MTT assay, to assess the viability of cells, and flow cytometric analysis, to measure apoptotic cell death, were performed, and the results, which revealed that the compound and pharmaceutically acceptable salts thereof have preventive and therapeutic activity against pancreatic cancer, are presented herein.

Abstract: Compounds useful for treating cellular proliferative diseases and disorders by modulating the activity of KSP are disclosed.

Abstract: A pyridazinone compound represented by the formula (I) have excellent effect on weed control and are useful as an active ingredient of herbicides.

Abstract: The present invention describes a process to form hydrazides from the reaction of a hydrazine and a dicarboxylic, using a Lewis acid as a main reagent of the reaction. The reaction occurs in a safe reactional environment, utilizing smooth conditions, neither involving high temperatures nor high pressures, producing the desired products with high yields, between 90-95%. The invention also describes a kit for utilization of chemiluminescent substances, comprised of two solutions.

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: An azole derivative of formula (I) a medicament that contains the azole derivative of formula (I), a method of treating a disease with the azole derivative of formula (I), and a method of preparing the azole derivative of formula (I).

Abstract: Compounds of formula wherein the substituents have the meanings given in claim 1, and agronomically tolerable salts, isomers and enantiomers of those compounds, are suitable for use as herbicides.

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: There is provided a combination product comprising; (A) melagatran or a pharmaceutically acceptable derivative thereof; and (B) dexamethasone or a pharmaceutically acceptable derivative there of, wherein each of components (A) and (B) is formulated in admixture with a pharmaceutically-acceptable adjuvant, diluent or carrier, as well as the use of such a combination product in the treatment of conditions including disseminated intravascular coagulation.

Abstract: The invention described herein relates to certain pyridazinedione N-substituted glycine derivatives of formula (I) which are antagonists of HIF prolyl hydroxylases and are useful for treating diseases benefiting from the inhibition of this enzyme, anemia being one example.

Abstract: Disclosed are sulfone compounds and compositions that inhibit soluble epoxide hydrolase (sEH), methods for preparing the compounds and compositions, and methods for treating patients with such compounds and compositions. The compounds, compositions, and methods are useful for treating a variety of sEH mediated diseases, including hypertensive, cardiovascular, inflammatory, pulmonary, and diabetes-related diseases.

Abstract: Disclosed are sulfonamide compounds and compositions that inhibit soluble epoxide hydrolase (sEH), methods for preparing the compounds and compositions, and methods for treating patients with such compounds and compositions. The compounds, compositions, and methods are useful for treating a variety of sEH mediated diseases, including hypertensive, cardiovascular, inflammatory, pulmonary, and diabetes-related diseases.

Abstract: Compounds useful for treating cellular proliferative diseases and disorders by modulating the activity of KSP are disclosed.

Abstract: The present invention relates generally to the field of anti-infective, anti-proliferative, anti-inflammatory, and prokinetic agents. More particularly, the invention relates to a family of compounds having both a biaryl moiety and at least one heterocylic moiety that are useful as such agents.

Abstract: The present invention describes pyridazinone compounds of formula I which are cyclooxygenase (COX) inhibitors, and in particular, are selective inhibitors of cyclooxygenase-2 (COX-2), COX-2 is the inducible isoform associated with inflammation, as opposed to the constitutive isoform, cyclooxygenase-1 (COX-1) which is an important “housekeeping” enzyme in many tissues, including the gastrointestinal (GI) tract and the kidneys. The selectivity of these compounds for COX-2 minimizes the unwanted GI and renal side-effects seen with currently markered non-steroidal anti-inflammatory drugs (NSAIDs).

Abstract: The invention relates to novel phenylpyridazinones of the general formula (I) in which R1, R2, R3, R4, R5 and R6 are each as defined in the description, to processes for their preparation, to their use as herbicides and to novel intermediates and processes for preparing them.

Abstract: The present invention describes pyridazinone compounds of formula I which are cyclooxygenase (COX) inhibitors, and in particular, are selective inhibitors of cyclooxygenase-2 (COX-2). COX-2 is the inducible isoform associated with inflammation, as opposed to the constitutive isoform, cyclooxygenase-1 (COX-1) which is an important “housekeeping” enzyme in many tissues, including the gastrointestinal (GI) tract and the kidneys. The selectivity of these compounds for COX-2 minimizes the unwanted GI and renal side-effects seen with currently marketed non-steroidal anti-inflammatory drugs (NSAIDs).

Abstract: The invention provides a process for synthesizing chlorinated pyrimidines. The process includes reacting imidoyl chloride compounds with phosgene (COCl2). The imidoyl chloride compounds can be supplied as starting materials or can be produced by reacting organic amides with phosgene or reacting organic nitrites with hydrogen chloride. Phosgene may be replaced by equivalent reagents. The chlorinated pyrimidines, such as 4,6-dichloropyrimidine, can be used to synthesize other compounds useful in a variety of compositions, such as fungicides, pesticides, and pharmaceuticals.

Abstract: A kit of parts containing (a) a pharmaceutical formulation including a low molecular weight thrombin inhibitor, or a pharmaceutically acceptable derivative thereof, in admixture with a pharmaceutically acceptable adjuvant, diluent or carrier, and (b) a pharmaceutical formulation including a prodrug of a low molecular weight thrombin inhibitor, or a pharmaceutically acceptable derivative of that prodrug, in admixture with a pharmaceutically acceptable adjuvant, diluent or carrier. Components (a) and (b) are each provided in a form that is suitable for administration in conjunction with the other. The kit is useful in the treatment of conditions in which inhibition of thrombin is required or desired.

Abstract: aP2 inhibiting compounds are provided having the formula wherein A, X, R and Z are as described herein. A method is also provided for treating diabetes and related diseases, especially Type II diabetes, employing such aP2 inhibitors alone or in combination with other therapeutic agents, including other antidiabetic agent such as metformin, glyburide, troglitazone and/or insulin.

Abstract: Compounds of formula wherein the substituents have the meanings given in claim 1, and agronomically tolerable salts, isomers and enantiomer of those compounds, are suitable for use as herbicides.

Abstract: Disclosed are compounds of the formula (I) or a pharmaceutically acceptable salt or solvate thereof. The compounds are useful for the treatment of chemokine-mediated diseases such as acute and chronic inflammatory disorders and cancer.

Abstract: There are described benzoylcyclohexanediones of the formula I, their preparation, and their use as herbicides and plant growth regulators. In this formula (I), C1, C2, C3 are cyclic radicals, X1 is a hetero atom, X2 is a chain of carbon atoms, L is a chain-like element, R1, R2, R3, R4, R5 are various radicals, and Y and Z are monoatomic bridge elements.

Abstract: The invention provides fungicidal compounds of formula (I) or stereoisomers thereof: wherein X is CH2O; A is hydrogen; E is hydrogen; q is 1; any two of K, L and M are nitrogen and the other is CH; T is oxygen or sulfur; and Z is an optionally substituted phenyl group or an optionally substituted heterocylyl group.

Abstract: This invention relates to novel sulfonyl pyridazinone compounds of the formula: wherein R1, R2, X, and Y are defined herein, which are useful as aldose reductase inhibitors in the treatment or prevention of certain complications arising from diabetes mellitus, pharmaceutical compositions comprising the sulfonyl pyridazinone, pharmaceutical compositions comprising a combination of the sulfonyl pyridazinone together with a second pharmaceutical agent, therapeutic methods comprising the administration of the sulfonyl pyridazinone compounds, therapeutic methods comprising the administration of the sulfonyl pyridazinone compounds in combination with a second pharmaceutical agent and compounds useful as intermediates for preparing the sulfonyl pyridazinone compounds of this invention.

Abstract: Methods for treating conditions associated with hyperglycemia, especially Type II diabetes, with novel naphthylsulfonic acids and related compounds. These compounds, as single stereoisomers or mixtures of stereoisomers, or their pharmaceutically acceptable salts, are useful in methods of stimulating the kinase activity of the insulin receptor, enhancing the activation of the insulin receptor by insulin, and stimulating the uptake of glucose into cells. A variety of antidiabetic compounds and pharmaceutical compositions comprising the antidiabetic compounds are also disclosed.

Abstract: The invention relates to novel phenylpyridazinones of the general formula (I) in which R1, R2, R3, R4, R5 and R6 are each as defined in the description, to processes for their preparation, to their use as herbicides and to novel intermediates and processes for preparing them.

Abstract: The present invention describes pyridazione compounds having the formula (I), which are cyclooxygenase (COX) inhibitors The compounds are selective inhibitors of cyclooxygenase-2-(COX-2), which is the inducible isoform associated with inflammation, as opposed to the constitutive isoform, cyclooxygenase-1 (COX-1), which is an important “housekeeping” enzyme in many tissues, including the gastrointestinal (GI) tract and the kidneys. The selectivity of these compounds for COX-2 minimizes the unwanted GI and renal side-effects seen with currently marketed non-steroidal anti-inflammatory drugs (NSAIDS).

Abstract: Phenylurethane compounds of the following general formula (1); asymmetric urea compounds of the following general formula (10) obtained from the phenylurethane compounds; barbituric acid derivatives of general formula (18) produced from the asymmetric urea compounds, which have specific substituents and are useful in diazo thermal recording materials; and diazo thermal recording materials containing the barbituric acid derivative.

Abstract: A pyridazinone derivative represented by formula (I): a pharmaceutically acceptable salt thereof, or a derivative thereof, or a pharmaceutical composition comprising as an active ingredient the derivative or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier or diluent.

Abstract: Novel pyridyl or pyrimidinyl substituted cycloalkenyl compounds and compositions for use in therapy.

Abstract: The present invention describes pyridazinone compounds of formula I 1

Abstract: The present invention describes pyridazinone compounds of formula I which are cyclooxygenase (COX) inhibitors, and in particular, are selective inhibitors of cyclooxygenase-2 (COX-2). COX-2 is the inducible isoform associated with inflammation, as opposed to the constitutive isoform, cyclooxygenase-1 (COX-1) which is an important “housekeeping” enzyme in many tissues, including the gastrointestinal (GI) tract and the kidneys. The selectivity of these compounds for COX-2 minimizes the unwanted GI and renal side-effects seen with currently marketed non-steroidal anti-inflammatory drugs (NSAIDs).

Abstract: A compound produced by the process comprising the step of reacting a starting compound of the formula: with FeCl3 in the presence of acetic acid, wherein the reaction mixture is heated and the temperature of the reaction mixture is about 85° C.to about reflux temperature, R1 and R2 in the above formula being as defined in the present specification.

Abstract: Substituted 2-phenyl-3(2H)-pyridazinones I and salts thereof, where n=0, 1, 2; R1=C1-C4-alkyl, C1-C4-haloalkyl; R2=H, halogen; R3=halogen, CN; R4=H, NO2, CN, CHO, NH—OH, C1-C4-alkyl, C1-C4-halogenalkyl, —OR5, —CH═N—OR6, —CH═C(R7)—CO—OR8, —CO—OR9, C1-C6-alkyl-SO2—NH, di(C1-C6-alkylsulfonyl)amino or R5=C1-C6-alkyl, C3-C6-alkenyl, C3-C6-alkynyl, (C1-C6-alkoxy)carbonyl-C1-C4-alkyl, (C3-C6-alkenyloxy)carbonyl-C1-C4-alkyl, (C3-C6-alkynyloxy)carbonyl-C1-C4-alkyl, C1-C4-alkoxy(C1-C4-alkoxy)carbonyl-C1-C4-alkyl; R6=H, C1-C4-alkyl, hydroxycarbonyl-C1-C4-alkyl, (C1-C4-alkoxy)carbonyl-C1-C4-alkyl; R7=H, halogen, C1-C4-alkyl; R8=H, C1-C6-alkyl; R9=H, C1-C6-alkyl, C3-C6-alkenyl, C3-C6-alkynyl, C1-C4-alkoxy-C1-C4-alkoxy, hydroxycarbonyl-C1-C4-alkyl, (C1-C6-alkoxy)carbonyl-C1-C4-alkyl, (C3-C6-alkenyloxy)carbonyl-C1-C4-alkyl, (C3-C6-alkynyloxy)car

Abstract: Imido and amido substituted alkanohydroxamic acids reduce the levels of TNF&agr; and inhibit phosphodiesterase in a mammal. A typical embodiment is 3-(3-cyclopentyloxy-4-methoxyphenyl)-N-hydroxy-3-phthalimidopropionamide.

Abstract: The present invention relates to a process for the preparation of compounds of the formula (I) by reacting compounds of the formula (II) in which Het, R1, R2 and R4 are as defined in the description, with urea.

Abstract: Compounds with fungicidal and insecticidal properties having formula I ##STR1## wherein W is ##STR2## n is 0 or 1; Y is O, S, NR.sub.1, or R.sub.6 ;the ring bond containing R.sub.4 and R.sub.5 is a single or double bond;X is independently selected from hydrogen, halo, (C.sub.1 -C.sub.4)alkyl, (C.sub.1 -C.sub.4)alkoxy and --HC.dbd.CH--CH.dbd.CH-- thereby forming a napthyl ring;R is independently selected from (C.sub.1 -C.sub.12)alkyl and halo(C.sub.1 -C.sub.12)alkyl;R.sub.1 is independently selected from (C.sub.1 -C.sub.12)alkyl, (C.sub.2 -C.sub.8)alkenyl and aryl;R.sub.2 is independently selected from hydrogen, (C.sub.1 -C.sub.12)alkyl (C.sub.1 -C.sub.12)alkoxy, halo(C.sub.1 -C.sub.12)alkyl, halo(C.sub.1 -C.sub.12)alkoxy, hydroxy(C.sub.1 -C.sub.12)alkyl, (C.sub.1 -C.sub.12)alkoxy(C.sub.1 -C.sub.12)alkyl, (C.sub.1 -C.sub.12)alkoxycarbonyl(C.sub.1 -C.sub.12)alkyl, (C.sub.2 -C.sub.8)alkenyl, halo(C.sub.2 -C.sub.8)alkenyl, (C.sub.3 -C.sub.10)alkynyl, halo(C.sub.3 -C.sub.10)alkynyl, (C.sub.3 -C.sub.

Abstract: The present invention relates to a process for producing a compound represented by the formula (II): ##STR1## wherein X is a halogen atom, each of A.sup.1, A.sup.2 and A.sup.3 are the same or different and are selected from a carbon atom or a nitrogen atom, provided that at least A.sup.1, A.sup.2, or A.sup.3 is a nitrogen atom. Each of R.sup.1, R.sup.2, R.sup.3 and R.sup.4 are the same or different and are selected from a hydrogen atom, a lower alkyl group, a cyano group, a carboxyl group, a lower alkoxycarbonyl group, a halogen atom, and a nitro group. It is also provided that where R.sup.1 and R.sup.2 are adjacent to each other, R.sup.1 and R.sup.2 may be combined with each other to form a 5- or 6-membered ring which may carry on the ring thereof one substituent selected from the group consisting of a lower alkyl group, a nitrile group, a carboxyl group, a lower alkoxycarbonyl group, a carbamoyl group, a halogen atom, a nitro group, and an amino-(lower alkyl) group.

Abstract: This application relates to compounds of the formula ##STR1## wherein R.sup.1,X, Y and n are as defined in the specification; and pharmaceutically acceptable addition salts thereof and optical and geometric isomers or racemic mixtures thereof; which compounds are useful for the treatment of various memory dysfunctions characterized by a decreased cholinergic function such as Alzheimer's disease. Compounds of this invention also inhibit monoamine oxidase and hence are useful as antidepressants.

Abstract: The invention encompasses the novel compound of Formula I as well as a method of treating cyclooxygenase-2 mediated diseases comprising administration to a patient in need of such treatment of a non-toxic therapeutically effective amount of a compound of Formula I. ##STR1## The invention also encompasses certain pharmaceutical compositions for treatment of cyclooxygenase-2 mediated diseases comprising compounds of Formula I.

Abstract: The present invention relates to cysteine protease inhibitors of the general formula (I): ##STR1## wherein Z is a cysteine protease binding moiety; X and Y are S, O or optionally substituted N; and R.sub.1 is optionally substituted alkyl or aryl.

Abstract: The invention relates to compounds of formula I and pharmaceutically acceptable salts and in vivo hydrolysable esters and amides thereof and processes for their preparation, their use as therapeutic agents and pharmaceutical compositions containing them. ##STR1## In formula I, A is a ring system in which the --CH(R.sup.3)N(R.sup.2)B--R.sup.1 and --OR.sup.4 groups are positioned in a 1,2 relationship to one another on ring carbon atoms. B is a ring system having R.sup.1 in a 1,3 or 1,4 relationship with the --CH(R.sup.3)N(R.sup.2)-- linking group. R.sup.2 is hydrogen or C.sub.1 -C.sub.6 -alkyl, R.sup.3 is hydrogen, methyl or ethyl, and R.sup.4 is C.sub.1 -C.sub.6 -alkyl, C.sub.1 -C.sub.6 -cycloalkyl-C.sub.1 -C.sub.3 -alkyl, C.sub.3 -C.sub.7 -cycloalkyl, N-oxides of --NR.sup.2, where chemically possible, or S-oxides of sulphur containing rings, where chemically possible. A, B, R.sup.1, R.sup.2, R.sup.3 and R.sup.4 may be substituted, as defined in the specification.

Abstract: Compounds of the formula ##STR1## inhibit endothelin, wherein: R is phenyl, naphthyl or biphenyl, each of which may be substituted.

Abstract: The, present invention relates to a novel allylthiopyridazine derivative represented by formula (I) which exhibits a superior effect for prevention and treatment or hepatic diseases induced by toxic substances and for protection of human tissues from radiation: ##STR1## or a pharmaceutically acceptable salt thereof, in which R.sub.1 represents halogen atom, lower alkoxy, dialkylaminoalkoxy, hydroxyalkoxy, phenoxy substituted or unsubstituted with lower alkyl, benzyloxy, or phenyl, andR.sub.2 and R.sub.3 independently of one another represent hydrogen or lower alkyl, or R.sub.2 and R.sub.3 together with carbon atom to which they are attached can form a saturated or unsaturated 6-membered ring,provided that R.sub.2 and R.sub.3 are other than hydrogen when R.sub.1 is chloro; and to a process for preparing thereof and a pharmaceutical composition containing the same as an effective component.