Abstract: The invention relates to compounds of Formula (I) wherein R1, (R2)v, R3 and n are defined in the specification and pharmaceutical compositions thereof, that inhibit the Ras farnesyl-protein transferase enzyme (FPTase), and may be used as an alternative to, or in conjunction with, traditional cancer therapy for the treatment of ras oncogene-dependent tumors, such as cancers of the pancreas, colon, bladder, and thyroid.

Abstract: Benzoxa- and benzthiazoles substituted at the 2 position and carrying a sulfamic acid ester group bound via oxygen to the phenyl part of the ring structure, such as the compounds of formula (I) wherein the symbols have various significances, possess interesting pharmacological activity. They can be prepared by sulfamoylation of a corresponding compound carrying a hydroxy group on the phenyl part of the ring structure, or by N-substitution. They are indicated for use as steroid sulfatase inhibitors in the prevention and treatment of illnesses responsive to steroid sulfatase inhibition, such as acne.

Abstract: Provided, among things, is a method of decreasing intraocular pressure in an animal, including a human, comprising administering an intraocular pressure decreasing amount of a compound of the formula I:

Abstract: The invention relates to the use of derivatives of E-type prostaglandins as EP2 agonists, in general, and, in particular as ocular hypotensives.

Abstract: The present invention provides a method of treating ocular hypertension or glaucoma which comprises administering to an animal having ocular hypertension or glaucoma therapeutically effective amount of a compound represented by the general formula I; wherein a hatched line represents the &agr; configuration, a triangle represents the &bgr; configuration, a straight line, e.g.

Abstract: A method of purifying an organic phosphoric ester characterized by treating a crude organic phosphoric ester with an epoxy compound and treating the treated organic phosphoric ester with an alkaline aqueous solution to purify it. The purification method is effective in stably obtaining an organic phosphoric ester reduced in acid value and excellent in heat resistance, hydrolytic resistance, and storage stability, regardless of the kind or amount of the organic phosphoric ester, the treating conditions, etc.

Abstract: The present invention relates to novel isothiazole derivatives of the formula wherein A represents a group selected from in which R1, R2, R3, R4, and R5 have the meanings given in the specification, to processes for the preparation of the novel compounds, and to their use as microbicides.

Abstract: The invention relates to a process for synthesizing piperazic acid and similar, ring-containing acids. The invention also relates to a process for simultaneously N(2)-acylating piperazic acid or an ester thereof and forming a bicyclic ring structure. The invention also relates to the use of either or both processes in a method of synthesizing a bicyclic compound useful as an intermediate for the production of an inhibitor of a caspase, particularly an inhibitor of interleukin-1&bgr; converting enzyme (“ICE”).

Abstract: Benzoylguanidines of the formula (I) in which R1 to R4 have the meanings given in the specification and claims are suitable as antiarrhythmic medicaments having a cardioprotective component for infarct prophylaxis and infarct treatment and for the treatment of angina pectoris. The compounds of the invention also preventively inhibit the pathophysiological processes in the formation of ischemically induced damage, in particular in the triggering of ischemically induced cardiac arrhythmias.

Abstract: A zwitterionic polyetherpolyamine comprising a linear or branched polyetherpolyamine backbone having 2 to 10 tertiary amino nitrogen atoms and a molecular weight of from 100 to 800, at least one tertiary amine end group of the polyetherpolyamine backbone contains two groups having the formula wherein A means an ethylene oxide unit, a propylene oxide unit, a unit of butylene oxides and a tetrahydrofuran unit, n is a number of from 1 to 50, X is an anionic group, with the proviso that in formula II one X may also be hydrogen and M is hydrogen, alkali metal or ammonium, or contains one group of formula I or II and one group selected from radicals consisting of C1- to C22-alkyl and C7- to c22-aralkyl, the meaning of A and n is the same as in formula I or II, said zwitterionic polyetherpolyamine having a molecular weight up to 9,000 and optionally containing up to 100% of the nitrogen atoms quaternized, and a process for the production of zwitterionic polyetherpolyamines by

Abstract: The present invention relates to a class of 2-aminothiazoline derivatives of formula I: in which either R1 is a hydrogen atom or an alkyl radical and R2 is an alkyl, -alk-NH2, —CH2—R3, —CH2—S—R4 or phenyl radical substituted with a nitro or —NH—C(═NH)CH3 radical, or R1 is an alkyl radical and R2 is a hydrogen atom, R3 is a (3-6C) cycloalkyl, pyridyl, pyridyl N-oxide, thienyl, thiazolyl, imidazolyl, pyrazinyl, triazolyl or phenyl radical or a phenyl radical substituted with a nitro, hydroxy or carboxyl radical, R4 represents a pyridyl or pyridyl N-oxide radical, alk represents an alkylene radical, or pharmaceutically acceptable salts thereof, which are useful as inhibitors of inducible NO-synthase.

Abstract: The present invention relates to a pharmaceutical composition for the hepatoprotection and treatment of liver diseases comprising as an active ingredient a dihydroxyphenyl derivative represented by the following formula (1), pharmaceutically acceptable acid addition salt or stereochemical isomer thereof together with a pharmaceutically acceptable inert carrier: in which in which A, B, D and E are defined as described in the specification.

Abstract: Compounds of formula (I): or a tautomeric form thereof, or a pharmaceutically acceptable salt thereof, or a pharmaceutically acceptable solvate thereof, wherein: A1 represents a substituted or unsubstituted aromatic heterocyclyl group; R1 represents a hydrocarbon atom, an alkyl group, an acyl group, an aralkyl group, wherein the aryl moiety may be substituted or unsubstituted, or a substituted or unsubstituted aryl group; R2 and R3 each represent hydrogen, or R2 and R3 together represent a bond; A2 represents a benzene ring having a total up to five substituents; and n represents an integer in the range of from 2 to 6; pharmaceutical compositions containing such compounds and the use of such compounds and compositions in medicine.

Abstract: Compounds of formula I are provided as well as pharmaceutically acceptable salts and esters thereof, wherein R1 to R5, n, m and A have the significance disclosed in the specification, and can be used for the treatment or prevention of arthritis, cardiovascular diseases, diabetes, renal failure, eating disorders and obesity.

Abstract: The present invention describes a novel method for the solid phase synthesis of polyamides containing imidazole and pyrrole carboxamides. The polyamides are prepared on a solid support from aromatic carboxylic acids and aromatic amines with high stepwise coupling yields (>99%), providing milligram quantities of highly pure polyamides. The present invention also describes the synthesis of analogs of the natural products Netropsin and Distamycin A, two antiviral antibiotics. The present invention also describes a novel method for the solid phase synthesis of imidazole and pyrrole carboxamide polyamide-oligonucleotide conjugates. This methodology will greatly increase both the complexity and quantity of minor-groove binding polyamides and minor-groove binding polyamide-oligonucleotide conjugates which can be synthesized and tested.

Abstract: The present invention provides organic dye compounds having their absorption maxima in a region ranging from the ultraviolet region to a relatively short wavelength visible region and uses thereof. The present invention provides specific monomethine cyanine dyes, light absorbents and optical recording media comprising the monomethine cyanine dyes, and a process for producing the monomethine cyanine dyes which comprises a step of reacting a quaternary ammonium salt of nitrogen atom-containing heterocyclic compound having a reactive methyl group with a quaternary ammonium salt of nitrogen atom-containing heterocyclic compound having an appropriate leaving group.

Abstract: A method of producing a compound of the formula: and its pharmaceutically acceptable salts, wherein Ar is a substituted or unsubstituted aromatic or heteroaromatic group; comprising: (1) reacting a compound of the formula: wherein Ar is as described above, with N2CHCOOR, wherein R is alkyl, in the presence of a catalytic amount of a Bronsted acid or Lewis acid to form a compound of the formula: wherein Ar and R are as described above; and (2) reacting the compound of formula (II) with a reducing agent in the presence of an alkyl amine to form a compound of the formula: wherein Ar and R are as described above.

Abstract: The invention relates to certain indolinone compounds, their method of synthesis, and a combinatorial library consisting of the indolinone compounds. The invention also relates to methods of modulating the function of protein kinases using indolinone compounds and methods of treating diseases by modulating the function of protein kinases and related signal transduction pathways.

Abstract: The present invention relates to novel aryl-substituted S(O)m cycles of the formula (I) in which F1, F2, G, V, W, X, Y, Z and m are each as defined in the description, to processes for their preparation and to their use in agriculture, for example as crop protection agents (fungicides, herbicides and insecticides).

Abstract: The present invention provides a method of treating ocular hypertension or glaucoma which comprises administering to an animal having ocular hypertension or glaucoma therapeutically effective amount of a compound represented by the general formula I; wherein hatched lines represent the &agr; configuration, a triangle represents the &bgr; configuration and a dotted line represents the presence or absence of a double bond; A and B are CH2; D represents a covalent bond or CH2, O, S or NH; X is CO2R, CONR2, CH2OR, P(O)(OR)2, CONRSO2R SONR2 or Y is O, OH, OCOR2, halogen or cyano; Z is CH2 or a covalent bond; R is H or R2; R1 is H, R2, phenyl, or COR2; R2 is C1-C5 lower alkyl or alkenyl and R3 is benzothienyl, benzofuranyl, naphthyl or substituted derivatives thereof, wherein the substituents maybe selected from the group consisting of C1-C5 alkyl, halogen, CF3, CN, NO2, NR2, CO2R and OR.