Abstract: The invention relates to dry powder formulations comprising respirable dry particles that contain 1) an antifungal agent in crystalline particulate form, 2) a stabilizer, and 3) one or more excipients.

Abstract: The present invention provides new class of 4?-[4?-(1?,3?-benzothiazole-2?-yl)anilino]podophyllotoxin analogues having the structural formula as follows (4). Where R?H or CH3; R1?H, halogen, CH3 and R2?H, halogen, OCH3. The present invention also provides a process for the preparation of new 4?-[4?-(1?, 3?-benzothiazole-2?-yl)anilino]podophyllotoxin analogues as useful anticancer agents. More particularly, it provides a process for the preparation of 4?-[4?-(1?,3?-benzothiazole-2?-yl)anilino] derivatives of podophyllotoxin. The process for the synthesis of new podophyllotoxin analogues as anticancer agents produces the novel and stereo-selective derivatives of the podophyllotoxin in good yields, where in the key step for the synthesis of these analogues is by direct nucleophilic substitution of C-4?-iodo intermediates.

Abstract: The invention relates a compound represented by the formula (1): Q1-Q2-C(?O)—N(R1)-Q3-N(R2)-T1-Q4??(1) wherein R1 and R2 represent H or the like; Q1 represents an aromatic ring, heterocyclic ring or the like; Q2 represents a single bond, aromatic ring, heterocyclic ring or the like; Q3 represents a group or the like, Q4 represents an aromatic ring, heterocyclic ring or the like; and T1 represents —CO— or —SO2—, and a medicine which comprises the compound and is useful for thrombosis and embolism.

Abstract: The present invention concerns compounds of formula (I), and pharmaceutically acceptable salts or solvates thereof, or solvates of such salts, 1

Abstract: The present invention relates to methods of treatment of certain metabolic diseases, and to novel compounds and their prodrugs, and/or pharmaceutically acceptable salts, pharmaceutical compositions containing such compounds useful in treating such diseases. In particular, this invention relates to the use of novel compounds and compositions for treatment of cardiovascular diseases, diabetes, cancers, acidosis, and obesity through the inhibition of malonyl-CoA decarboxylase (MCD). These compounds have the formulae (I) and (II), wherein Y, C, R1, R2, R6, and R7 are defined herein.

Abstract: The invention provides compounds of formula 1,

Abstract: The present invention provides novel compounds represented by the general formula I.

Abstract: The present invention relates to processes for the conversion of nitrites to amidines in the preparation of compounds which are antagonists of the platelet glycoprotein IIb/IIIa fibrinogen receptor complex. The compounds described herein are potent thrombolytics and useful for the inhibition of platelet aggregation in the treatment of thromboembolic disorders.

Abstract: There are provided 1-(3-heterocyclyphenyl)isothiourea, -isourea, -guanidine and -amidine compounds of formula I 1

Abstract: An improved process is provided for preparing water-soluble prodrugs of triazole antifungal compounds containing a secondary or tertiary hydroxyl group.

Abstract: Water-soluble prodrugs of triazole antifungal compounds having a secondary or tertiary hydroxy group are provided.

Abstract: Novel polythiophene-containing structural units of the general formulae (I) and (II) processes for their preparation, monomers for their preparation, their use in various industrial fields, and an electrically conductive material comprising these.

Abstract: The invention encompasses compounds of Formula I as well as a method of treating COX-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. The invention also encompasses certain pharmaceutical compositions for treatment of COX-2 mediated diseases comprising compounds of Formula I.

Abstract: N-Benzylazolium derivatives of the general formula (I), ##STR1## wherein Q is the remainder of an azole compound of the formula II ##STR2## possessing antifungal activity; Z is nitrogen or methine;R.sup.1 and R.sup.2 are each independently a hydrogen atom or a group --OY ?in which Y is a group easily hydrolyzable under physiological condition!;R.sup.3 and R.sup.4 are each independently a hydrogen or halogen atom, lower alkyl, lower alkoxy, lower alkylthio, (lower alkylcarbonyl)thiomethyl, carboxy or methoxycarbonyl; andX.sup.- is a pharmaceutically acceptable anion,as well as salts, hydrates or solvates of the compounds of the general formula (I) have antifungal properties.

Abstract: Compounds of formula ##STR1## wherein R, R.sub.1, R.sub.2, R.sub.3, R.sub.4 and n have the meanings reported in the description are described.The compounds of formula I are endowed with a dual ACE-inhibitory and NEP-inhibitory activity and are useful in the treatment of cardiovascular diseases.

Abstract: [Object]To provide a new 2,4-oxazolidinedione derivative possessing excellent hypoglycemic and hypolipidemic activities.[Constituent]A 2,4-oxazolidinedione derivative represented by the general formula: ##STR1## wherein X represents --CH.sub.2 --, --C(.dbd.O)--, --CH(OH)--, --C(.dbd.NOH)-- or --CH.dbd.CH--; R represents a hydrocarbon residue or heterocyclic group which may be substituted; n represents an integer from 0 to 5, and m represents an integer from 1 to 3; ....... represents a single or double bond; provided that n is an integer from 1 to 5 when X is --C(.dbd.O)--, or a pharmacologically acceptable salt thereof.

Abstract: The internally cyclized congeners of hydroxy-substituted nucleotide analogues have been found to exhibit substantially lower toxicity in vivo than their uncyclized analogues, while retaining essentially the same antiviral activity. This was unexpected because the prior art suggested that the cyclic analogues offered no significant advantages in respect to toxicity. This finding permits the administration of much greater doses of the cyclic congeners than otherwise would have been possible and allows the clinician to omit toxicity ameliorating interventions. Novel compounds are provided for use in the method of this invention. Novel methods for the preparation of these compounds also are provided.

Abstract: This invention relates to a compound represented by the formula: ##STR1## wherein B represents a hydrogen atom or a lower alkyl group; ring A represents a benzene ring which may have one or more substituents; .multidot..multidot..multidot..multidot..multidot. represents a single or double bond; Q.sub.1 represents the group represented by the formula, ##STR2## or a hydrocarbon residue substituted with the group represented by the formula, ##STR3## wherein X represents a bond or a spacer having a chain length of 1 to 4 atoms as the linear moiety which may have one or more side chains; R.sup.1 and R.sup.2, whether identical or not, independently represent a hydrogen atom or a lower alkyl, or may bind together to form a ring; Q.sub.2 represents a hydrogen atom, a hydrocarbon residue which may be substituted or a heterocyclic ring residue which may be substituted; or a salt thereof.

Abstract: The invention provides compounds of formula (I): ##STR1## or a physiologically acceptable salt, solvate or metabolically labile ester thereof whereinR.sup.1 represents a hydrogen atom or a halogen atom or a group selected from C.sub.1-6 alkyl, C.sub.2-6 alkenyl, fluoroC.sub.1-6 alkyl, C.sub.1-6 alkoxy, --CHO, --CO.sub.2 H or --COR.sup.2 ;Ar represents the group ##STR2## Het represents an N-linked imidazolyl group optionally substituted by one, two or three substituents.The compounds may be used in the treatment or prophylaxis of hypertension and diseases associated with cognitive disorders.

Abstract: Oxazole derivatives having Formula I or II are disclosed which are useful as inhibitors of mammalian blood platelet aggregation. ##STR1## Formula I and Formula XIX compounds are those wherein n is 7-9 and R is hydrogen or lower alkyl. Formula II compounds are those wherein R is hydrogen, lower alkyl or together with CO.sub.2 is tetrazol-1-yl; R.sub.1 is phenyl or thienyl; X is a divalent connecting group selected from the group consisting of CH.sub.2 CH.sub.2, CH.dbd.CH, and CH.sub.2 O; Y is a divalent connecting group attached to the 3 or 4 phenyl position selected from the group consisting of OCH.sub.2, CH.sub.2 CH.sub.2 and CH.dbd.CH. Formula XX compounds are those wherein the OCH.sub.2 CO.sub.2 R moiety is attached to the 3 or 4 phenyl position and R is hydrogen or lower alkyl.

Abstract: A phosphorylating agent represented by the following general formula [1]: ##STR1## wherein R represents a protective group of the phosphoric acid; and X represents a heterocyclic residue represented by the following general formula [2]: ##STR2## wherein Y represents a single bond or an oxygen or sulfur atom; Z represents a heterocyclic nucleus comprising at least one nitrogen atom as a ring-forming element and may be condensed with another aromatic ring; and W represents one or more substituents other than a hydrogen atom. The phosphorylating agent is stable, can rapidly proceed phosphodiester bond-forming reactions in good selectivity under mild conditions and thus makes it possible to perform a reaction even in a relatively large scale.

Abstract: Lipid derivatives represented by the formula: ##STR1## wherein R.sup.1 stands for an optionally substituted higher alkyl group, R.sup.2 stands for an optionally substituted lower alkyl group or an optionally substituted nitrogen-containing heterocyclic group, R.sup.3 stands for a tertiary amino group or a quaternary ammonium group, J stands for oxygen atom or S(O)t (where t deontes 0, 1 or 2), m and n respectively denotes 1 or 2, p denotes 0, 1 or 2, q and r respectively denote an integer of 2 to 5.and salts thereof have antitumor activities including differentiation-inducing activity and are useful as antitumor agents.

Abstract: A compound represented by the formula: ##STR1## wherein R represents a hydrogen atom or a lower alkyl group;R.sup.1 represents a higher alkyl group which may be substituted;R.sup.2 represents a hydrogen atom or a lower alkyl group, a lower alkanoyl group or a nitrogen-containing 5- to 7-membered heterocyclic group each of which may be substituted; X represents a divalent group represented by the formula:--(OCH.sub.2 CH.sub.2).sub.p --wherein p represents an integer of 1 to 5, a divalent group represented by the formula:--O(CH.sub.2).sub.q --wherein q represents an integer of 3 to 8, or a divalent group represented by the formula:--(OCH.sub.2 CH.sub.2).sub.p --J--(CH.sub.2).sub.q --wherein J represents an oxygen atom or a group represented by the formula: --S(O).sub.

Abstract: Novel alkoxycarbonylalkylphospholipids, alkylaminocarbonylalkylphospholipids, processes for the preparation thereof, and methods for treating inflammation utilizing compounds or compositions thereof are disclosed.

Abstract: In the preparation of a (thiono)phosphoric ester of the formula ##STR1## in which X represents oxygen or sulphur,R and R.sup.1 are identical or different and represent alkyl, andR.sup.2 represents optionally substituted aryl or represents optionally substituted hetaryl having at least one nitrogen atom,wherein a hydroxyl derivative of the formulaR.sup.2 --OHor an ammonium, alkali metal or alkaline earth metal salt thereof is reacted with a (thiono)phosphoric halide of the formula ##STR2## in which Hal represents halogen,the improvement which comprises effecting the reaction in the presence of a bicyclic organic amine as catalyst. Advantageously the reaction is effected in a diluent in the presence of potassium carbonate as an acid acceptor at 20.degree. to 100.degree. C., and 0.8 to 1.5 mols of the halide and 0.005 to 0.5 mol of 1,4-diazabicayclo-(2,2,2)-octane are used as bicyclic organic amine per mol of the hydroxyl compound.

Abstract: Compounds of the formula ##STR1## in which one of the symbols R.sub.1 and R.sub.2 represents an alkyl radical that has 3 or 4 carbon atoms and is unsaturated in the 2,3-position, and the other represents such a radical or lower alkyl, R.sub.3 and R.sub.4 each represents, independently of the other, hydrogen or methyl, and A represents a radical of the formula ##STR2## in which Z.sub.1, or each of Z.sub.2 and Z.sub.3 independently of the other, represents hydrogen or lower alkyl, or Z.sub.2 and Z.sub.3 together represent lower alkylene, each of R.sub.5 and R.sub.6, independently of the other, represents hydrogen, lower alkyl, halogenated lower alkyl, or lower alkenyl or R.sub.5 and R.sub.6 together represent lower alkylene that is optionally interrupted by oxygen, sulphur or by optionally substituted nitrogen, and X represents OR.sub.7 or NR.sub.8 R.sub.9 in which R.sub.7 represents hydrogen or lower alkyl and each of R.sub.8 and R.sub.

Abstract: This invention relates to phosphoroamidothioate and phosphorcamidodithioate compounds, to compositions thereof which are useful as pesticides. For example, as arthropodicides (that is, insecticides and acaricides), nematocides, and fungicides, and to a method of controlling pests, such as insects, acarids, nematodes, and fungi. The compounds of the invention are effective against soil insects, especially the corn rootworm, when applied by soil application techniques and are also effective when applied to agricultural plants and other plants by foliar application techniques.

Abstract: Compounds of the formula ##STR1## in which one of the symbols R.sub.1 and R.sub.2 represents an alkyl radical that has 3 or 4 carbon atoms and is unsaturated in the 2,3-position, and the other represents such a radical or lower alkyl, R.sub.3 and R.sub.4 each represents, independently of the other, hydrogen or methyl, and A represents a radical of the formula ##STR2## in which Z.sub.1, or each of Z.sub.2 and Z.sub.3 independently of the other, represents hydrogen or lower alkyl, or Z.sub.2 and Z.sub.3 together represent lower alkylene, and salts of such compounds in which Z.sub.1, or Z.sub.3 and optionally also Z.sub.2, represent(s) hydrogen, exhibit tumor-inhibiting activities.

Abstract: A multifunctional ashless additive is described having antiwear and antioxidant properties and high antirust power, and is prepared by reacting a O,O'-dialkylthiophosphoric acid with a compound chosen from substituted 2-oxazolines and substituted imidazolines.

Abstract: A method of protecting plants from plant parasitic nematodes is provided. This method comprises applying to the locus of nematode infestation a plant protective amount of a mixture consisting essentially ofA. O,O-diethyl O-(5-phenylisoxazol-3-yl)phosphorothioate, andB. at least one of:(1) methyl N-[[(methylamino)carbonyl]oxy]ethanimidothioate,(2) methyl 2-(dimethylamino)-N-[[(methylamino)carbonyl]oxy]-2-oxoethanimidothioate; and(3) 2-methyl-2-(methylthio)propionaldehyde O-methylcarbamoyloxime,the weight ratio of A to B being in the range of about 1:10 to about 10:1, preferably about 2:1 to about 3:1.

Abstract: Compounds having the structures: ##STR1## wherein B is A or a hydrogen and A is R--X; wherein X is ##STR2## M is a Group II metal cation and R is a hydrocarbyl group having about 1 to 100 carbon atoms.