Abstract: The present invention relates to a process preparing compounds of the general formula (I) 1

Abstract: The present invention relates to novel heterocyclyl-containing diaryl sulfide compounds that are useful for treating inflammatory and immune diseases, to pharmaceutical compositions comprising these compounds, and to methods of inhibiting inflammation or suppressing immune response in a mammal.

Abstract: The invention relates to heterocyclic derivatives of formula (I) and (Ia), or pharmaceutically-acceptable salts thereof, which possess antithrombotic and anticoagulant properties and are accordingly useful in methods of treatment of humans or animals. The invention also relates to processes for the preparation of the heterocyclic derivatives, to pharmaceutical compositions containing them and to their use in the manufacture of medicaments for use in the production of an antithrombotic or anticoagulant effect.

Abstract: Compounds of the formula: useful in the treatment of arthritis, tumor metastasis, tissue ulceration, abnormal wound healing, periodontal disease, bone disease, diabetes (insulin resistance) and HIV infection.

Abstract: Matrix metalloproteinases (MMPs) are a group of enzymes that have been implicated in the pathological destruction of connective tissue and basement membranes. These zinc containing endopeptidases consist of several subsets of enzymes including collagenases, stromelysins and gelatinases. TNF-&agr; converting enzyme (TACE), a pro-inflmatory cytokine, catalyzes the formation of TNF-&agr; from membrane bound TNF-&agr; precursor protein. It is expected that small molecule inhibitors of MMPs and TACE therefore have the potential for treating a variety of disease states.

Abstract: Compounds characterized generally as ethynyl alanine amino diol derivatives are useful as renin inhibitors for the treatment of hypertension.

Abstract: A phenothiazine, acridan, acridone oxime, acridone hydrazone and dibenzodiazepine derivative represented by formula (I) effective against diseases in which histamine, leukotrienes, etc. participate and effective in preventing or treating diseases in which chemical mediators such as histamine and leukotrienes participate, for example, asthma, allergic rhinitis, atopic dermatitis, urticaria, hay fever, gastrointestinal allergy and food allergy.

Abstract: Novel carboxamide derivatives having CNS activity, processes for their preparation and their use as medicaments

Abstract: Novel sulfidoamidocarboxylic acids (salts), a method for the production thereof, and uses therefor are provided. Sulfidoamidocarboxylic acids (salt) with a thiazolidine residue such as dimethylthiazolidine or methylthiazolidine or thiazolidine residue (residues), or a polycarboxylic acid (salt) residue such as dicarboboxylic acid (salt) or tricarboxylic acid (salt) or tetracarboxylic acid (salt) residue, a method for the production thereof, and uses therefor are also provided.

Abstract: The present invention relates to cyclic sulfone moiety-containing hydroxyethylamine protease inhibitor compounds and pharmaceutical or method of use therefor, particularly as an inhibitor of HIV protease.

Abstract: This invention provides a convenient, new, one step process for the preparation of 2-(trihaloacetyl)-3-(substituted amino)-2-propenoates and related derivatives thereof by reaction of carbonyl compounds substituted with a trihaloacetyl group with an acetal in the presence of an organic acid. The resulting propenoates are useful as intermediates for the construction of trihalomethyl substituted heterocyclic compounds for use in pharmaceutical and agricultural applications.

Abstract: A compound according to the formula (I) wherein R1 and R2 are independently the atoms necessary to complete the formation of a substituted or unsubstituted aromatic or aliphatic carbocyclic or heterocyclic ring system and R3 and R4 have the meaning indicated in claim 1, a new process for the preparation of such a compound, solid solutions and mixtures comprising such a compound and the use of a compound of formula (I) as a pigment.

Abstract: The present invention relates to novel substituted phenols and derivatives thereof useful in the treatment of neurological disorders. Methods of preparing the compounds, intermediates useful in the preparation and pharmaceutical compositions containing the compounds are also includes.

Abstract: This invention relates to peptide derivatives, pharmaceutical formulations containing those compound and methods of their use as thrombin inhibitors.

Abstract: The present invention provides novel compounds, compounds and pharmaceutical compositions thereof, and methods of using same in the treatment of affective disorders, anxiety, depression, post-traumatic stress disorders, eating disorders, supranuclear palsy, irritable bowel syndrome, immune suppression, Alzheimer's disease, gastrointestinal diseases, anorexia nervosa, drug and alcohol withdrawal symptoms, drug addiction, inflammatory disorders, or fertility problems. The novel compounds provided by this invention are those of formula: ##STR1## wherein R.sup.1, R.sup.3, R.sup.4, R.sup.5, Z, Y, V, X, X', J, K, L, and M are as defined herein.

Abstract: Compound of formula (I): ##STR1## wherein: Y, R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, R.sub.6, R.sub.7, R.sub.8 and n are as defined in the description, and medicinal products containing the same which are useful as imidazoline receptor ligands.

Abstract: Spin trapping compositions in general have now been discovered to be effective in treating a variety of disorders, including disorders such as those arising from ischemia, infection, inflammation, exposure to radiation or cytotoxic compounds, not just of the central and peripheral nervous systems but of peripheral organ disease having a wide variety of etiologies. In the preferred embodiment, the compositions for treating tissue damage from ischemia contain PBN, or active derivatives thereof, in a suitable pharmaceutical carrier for intravenous, oral, topical, or nasal/pulmonary administration. Other preferred spin-trapping agents include 5,5-dimethyl pyrroline N-oxide, (DMPO), .alpha.-(4-pyridyl-1-oxide)-N-tert-butylnitrone, (POBN), and (TEMPO) spin-trapping derivatives thereof. Examples of derivatives of PBN include halogenated derivatives, bifunctional derivatives, conjugates with drugs or targeting molecules, dimers and cyclodextran polymers of PBN.

Abstract: The compounds of Formula I ##STR1## are useful as immunosuppressive agents.

Abstract: The novel compounds of formula I: ##STR1## (R.sup.1, R.sup.2, R.sup.3, L.sup.1, L.sup.2 and Hal are defined in the specification) show selective fungicidal activity. These compounds may be processed with carriers, and optionally an adjuvant, to produce fungicidal compositions.

Abstract: The invention relates to novel bis-benzimidazole compounds which have the ability to bind to the minor groove of DNA and to alkylate DNA, to methods of preparing the compounds, and the use of the compounds in the treatement of neoplastic disease.

Abstract: Disclosed are compounds of the formula I wherein:Y represents --CO.sub.2 H, --CO.sub.2 R.sup.6, --C(O)NHR.sup.7, --SO.sub.2 H, --SO.sub.3 H, --SO.sub.3 R.sup.6, --SO.sub.2 NHR.sup.7, --C(O)--N(OH)--R.sup.8, or a group of the formula ##STR1## or a pharmaceutically acceptable addition salt or solvate thereof. Also disclosed are pharmaceutical compositions containing compounds of Formula I. Further disclosed is a method for treating or preventing respiratory depression, epileptic seizures or other central nervous system disorders, and for enhancing cognitive performance, by administering an effective amount of a compound of Formula I.

Abstract: This invention relates to a 1,2-ethanediol derivative and a salt thereof, a process for producing the same, and a cerebral function-improving agent comprising the same. The cerebral function-improving agent of this invention is useful for treating cerebrovascular dementia, senile dementia, Alzheimer's dementia, sequelae of ischemic encephalopathy and cerebral apoplexy.

Abstract: The present invention relates to indole derivatives represented by the following compound 1 and the pharmacologically acceptable acid addition salt thereof. ##STR1## The compounds of the present invention were found to exhibit strong antitussive and analgesic actions as a result of pharmacological evaluation, and can be used in the pharmaceutical field as effective antitussives and analgesics.

Abstract: Novel tricyclic heterocyclic sulfonamide derivatives and sulfonic ester derivatives which have each an antitumor action and are represented by the following general formula (I) and processes for producing the same are provided. These compounds have each an excellent antitumor activity.A sulfonamide derivative or a sulfonic ester derivative represented by the following general formula (I): ##STR1## {G represents an aromatic 5- or 6-membered ring; L represents 0 or --N(R.sup.1)-- (R.sup.1 represents hydrogen or lower alky); and M represents a tricyclic structure selected from among the following ones; ##STR2## ?rings A and B represent each an unsaturated 5- or 6-membered ring; X represents N(R.sup.2), (wherein R.sup.2 represents hydrogen or lower alkyl), or NHCO;Y represents O, S(O).sub.n, C(R.sup.3)(R.sup.4), C(O), N(R.sup.5), CH(R.sup.6)CH(R.sup.7), C(R.sup.8).dbd.C(R.sup.9), N(R.sup.10)C(O), N.dbd.C(R.sup.11), OCH(R.sup.12), S(O).sub.n CH(R.sup.13) or N(R.sup.14)CH(R.sup.15);Z represents nitrogen or C(R.sup.

Abstract: The invention provides hydroxamic acid derivatives of the general formula ##STR1## wherein R.sup.1 represents cyclopropyl, cyclobutyl, cyclopentyl or cyclohexyl; R.sup.2 represents a saturated 5- to 8-membered monocyclic or bridged N-heterocyclic ring, which N-heterocyclic ring is attached via the N atom and when it is monocyclic, optionally contains NR.sup.4, O, S, SO or SO.sub.2 as a ring member and/or is optionally substituted on one or more C atoms by hydroxy, lower alkyl, lower alkoxy, oxo, ketalized oxo, amino, mono(lower alkyl)amino, di(lower alkyl)amino,carboxy, lower alkoxycarbonyl, hydroxy-methyl, lower alkoxymethyl, carbamoyl, mono(lower alkyl)-carbamoyl, di(lower alkyl)carbamoyl or hydroxyimino; R.sup.3 represents a 5- or 6-membered N-heterocyclic ring which (a) is attached via the N atom, (b) optionally contains N, O and/or S, SO or SO.sub.

Abstract: Novel aminoalkyloximes, precursors and processes for the preparation thereof, and methods of treating depression and obsessive compulsive disorders are described.

Abstract: Novel aminoalkyloximes, precursors and processes for the preparation thereof, and methods of treating depression and obsessive compulsive disorders are described.

Abstract: Novel aminoalkyloximes, precursors and processes for the preparation thereof, and methods of treating depression and obsessive compulsive disorders are described.

Abstract: Novel aminoalkyloximes, precursors and processes for the preparation thereof, and methods of treating depression and obsessive compulsive disorders are described.

Abstract: Novel aminoalkyloximes of the formula ##STR1## wherein: a. X is hydrogen, loweralkyl, loweralkoxy, halogen, trifluoromethyl, or a group of the formula ##STR2## wherein Y is hydrogen or loweralkyl, and p is 1 or 2; b. A is a group of the formula ##STR3## c. R.sup.1 and R.sup.2 are independently hydrogen or lowerakyl; and d. m is 2 to 6 and n is 0, or 2 to 6, inclusive, serotonin reuptake inhibitors, useful for treating depression and obsessive compulsive disorders are described. Also described are precursors of and processes for the preparation of such aminoakyloximes.

Abstract: Novel carbostyril derivatives of the formula: ##STR1## wherein R.sup.1 is H, NO.sub.2, alkoxy, alkoxycarbonyl, alkyl, halogen, optionally substituted amino, OH, CN, COOH, alkanoyloxy, hydrazinocarbonyl; q is 1 to 3, and R is a group of the formula: ##STR2## [wherein R.sup.2 is H, alkoxycarbonyl, optionally substituted phenoxycarbonyl, phenylalkenyl-CO--, optionally substituted phenylalkanoyl, alkanoyl, alkenyl-CO--, optionally substituted phenyl-SO.sub.2 --, --CONR.sup.8 R.sup.9, optionally substituted heterocyclic group-CO--, naphthyl-CO--, thienylalkanoyl, tricyclo[3.3.1.1]alkanoyl, ##STR3## (R.sup.13 is OH, optionally substituted alkoxy, --NR.sup.32 R.sup.33, --O--A--(E).sub.l --NR.sup.4 R.sup.5, --(B).sub.l --NR.sup.6 R.sup.7, etc.),n is 1 or 2, m is 0 or 1 to 3, R.sup.3 is alkyl, R.sup.10 is --(CO).sub.l --NR.sup.11 R.sup.

Abstract: Compounds structurally related to ethacrynic acid are described. The compounds are useful for controlling intraocular pressure. Unlike ethacrynic acid, the compounds of the present invention are capable of effectively penetrating the cornea. Methods of controlling intraocular pressure via topical application of one or more of the compounds to the eye and topical ophthalmic compositions useful in the treatment of glaucoma are also described.

Abstract: Compounds of formula (I): ##STR1## [wherein: R.sup.1 is a cyclic amino group, or a dialkylamino group; R.sup.2 a group of formula --NHCHR.sup.3 R.sup.4 wherein R.sup.3 and R.sup.4 are each alkyl aryl or aralkyl, or together form a cycloalkyl group, or R.sup.2 is an aromatic heterocyclic group, or a group of formula --B--S(O).sub.m --R.sup.5 wherein R.sup.5 is a substituted alkyl group, or an aromatic heterocyclic group; B is an alkylene or alkylidene group; m is 0, 1 or 2; A is a group of formula --CH.dbd.CH-- or --(CH.sub.2).sub.n --, where n is 1, 2 or 3]; and salts thereof have valuable anti-ulcer activity.

Abstract: This invention relates to certain triazolopyrimidine derivatives of formula I ##STR1## wherein R.sub.1 represents an optionally substituted alkyl, alkenyl, alkynyl, alkadienyl, cycloalkyl, bicycloalkyl or heterocyclyl group; R.sub.2 represents a hydrogen atom or an alkyl group; or R.sub.1 and R.sub.2 together with the interjacent nitrogen atom represent an optionally substituted heterocyclic ring; R.sub.3 represents an optionally substituted aryl group; and R.sub.4 represents a hydrogen or halogen atom or a group --NR.sub.5 R.sub.6 where R.sub.5 represents a hydrogen atom or an amino, alkyl, cycloalkyl or bicycloalkyl group and R.sub.6 represents a hydrogen atom or an alkyl group; processes for their preparation; compositions containing such compounds and their use as fungicides.

Abstract: This invention relates to the compounds of the formula [I] which are useful for the treatment of cataracts, and the synthetic intermediates of the formula [II], ##STR1## wherein R.sup.1 is hydroxy which can be protected by a hydroxy protective group;R.sup.2 is lower alkyl;R.sup.3 is hydrogen, lower alkyl, hydroxy, which can be protected by a hydroxy protective group, or lower alkoxy, and the said lower alkyl can be substituted by hydroxy, which can be protected by a hydroxy protective group, amino or lower alkylamino;R.sup.4 is carboxy which can be converted into ester or amide; tetrazolyl; phosphono which can be converted into ester or amide; or sulfonyl which can be converted into ester or amide;R.sup.5 is cyano or lower alkoxy;A is alkylene;B is C.dbd.O, C.dbd.S or CH.sub.2, andis single bond or double bond.

Abstract: Compounds of formula I ##STR1## wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5 and A-B have any of the meanings given in the specification, and their pharmaceutically acceptable salts are useful in the treatment of urinery incontinence. Also disclosed are pharmaceutical compositions, processes for preparing the compounds of formula I and intermediates.

Abstract: Disclosed are compounds of the formula: ##STR1## wherein: A represents arylalkyl, aryl or heteroaryl; X is nitrogen or CH; and R.sub.2, R.sub.3, R.sub.4 and R.sub.5 represent organic or inorganic substituents;and the pharmaceutically acceptable salts thereof; useful for treating disorders of the central nervous system.

Abstract: Arthropodicidal compounds, compositions and arthropodicidal use of compounds having the formula ##STR1## wherein A, X, R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, m and n are as defined in the text.

Abstract: Compounds of formula I ##STR1## and their salts in which R.sub.1 is optionally substituted phenyl, R.sub.2 is alkyl, cycloalkyl or optionally substituted amino, or R.sub.2 and R.sub.3 together with the nitrogen and carbon atoms to which they are attached form an optionally substituted heterocyclic ring or R.sub.3 and R.sub.4 together with the nitrogen atom to which they are attached form an optionally substituted heterocyclic ring and R.sub.5 is H, halo, alkyl, alkoxy, trifluoromethyl or a group of formula S(O).sub.m R.sub.8 in which m is 0, 1 or 2 and R.sub.8 is alkyl have utility in the treatment of diabetes particularly in the treatment of hyperglycaemia.

Abstract: Metal-free compounds of the formula ##STR1## a 1:1 or 1:2 metal complex of a metallizable compound of said formula or a salt of a metal-free compound of said formula or of a 1:1 or 1:2 metal complex thereof each cation of which is independently a non-chromophoric cation, or a mixture, thereof, whereinF.sub.c is the radical of a water-soluble azo, formazan, phthalocyanine, azomethine, oxazine, thiazine, phenazine or triphenylmethane dye,each W is independently --NR.sub.1 --B.sub.1 --NR.sub.1 --, ##STR2## wherein B.sub.1 is linear or branched C.sub.2-6 alkylene; linear or branched C.sub.2-6 alkylene interrupted by --O-- or --NR.sub.1 --; linear or branched C.sub.3-6 alkylene monosubstituted by hydroxy or carboxy or disubstituted by hydroxy, ##STR3## wherein R.sub.2 is hydrogen, C.sub.1-4 alkyl, C.sub.1-4 alkoxy, carboxy or sulfo, andn is 0, 1, 2, 3 or 4, andm is 0 or 1,each X is independently a direct bond, --CO-- or --SO.sub.

Abstract: Substituted 1,2,4-triazolo[1,5-c]pyrimido[1,4]azines have been found to have potent bronchodilator activity. Pharmacological methods for inducing bronchodilation using such compounds, pharmaceutical compositions containing such compounds, and synthetic intermediates for preparing such compounds are also described.

Abstract: Novel 3-pyrrolidinylthio-1-azabiycyclo[3.2.0]hept-2-ene-2-carboxylic acid compounds and pharmaceutically acceptable salts thereof have antimicrobial activity and are useful as medicaments in the treatment of infectious diseases caused by pathogenic microorganisms.

Abstract: Thioacids, thiols, an acid, and an aldehyde are used to produce chiral thioacetals of the general formula. ##STR1## The compounds are leukotriene antagonists.

Abstract: A composition for thrombolytic therapy includes a tissue-type plasminogen activator (t-PA) and a low affinity heparin fraction. The composition is administered intravenously to allow the t-PA to dissolve blood clots while the low affinity heparin fraction prevents reocculsion without the harmful side effects observed for unfractionated heparin, such as, stimulation of and interference with t-PA activity in the circulatory system, as well as, interference with fibrinolytic activity which can cause hemorrhaging in the mammalian circulatory system.

Abstract: There is provided a pest control composition containing a compound represented by the formula, ##STR1## wherein R.sup.1, R.sup.2, R.sup.3 and R.sup.4 are the same or different and independently mean a hydrogen atom, a hydrocarbon group which may be substituted or a heterocyclic group which may be substituted and X means an electron attracting group or a salt thereof.The compounds are of minimal toxicity to man, domestic animals and fish and selectively display remarkable control effect on pests.

Abstract: [(Bicyclic heterocyclyl)methyl and --hetero] substituted hexahydro--1H--azepines and pyrrolidines and their pharmaceutically acceptable acid addition salts having anti--histaminic properties, compositions containing the same, and methods of treating allergic diseases in warm-blooded animals.

Abstract: Pyrimidine compounds useful as plant growth regulators have the formula (I): ##STR1## wherein Y is an optionally substituted secondary or tertiary alkyl group containing from 3 to 7 carbon atoms or an optionally substituted cycloalkyl or alkylcycloalkyl group containing from 3 to 7 carbon atoms; R.sup.1 and R.sup.2, which may be the same or different, are hydrogen or a lower alkyl group; A is an optionally substituted heterocyclic group, for example thienyl or pyridyl; n is an integer which may be from 0 to 2 and is preferably 0; and R.sup.3 is hydrogen, an alkyl group containing from 1 to 4 carbon atoms, or an alkenyl or alkynyl group containing from 2 to 4 carbon atoms.

Abstract: Gem 3 dialkyl or spiro 4 aryl or heteroaryl 5 heterocyclic 3 H indoles and their pharmaceutically acceptable salts are prepared. They are useful for reducing blood pressure producing a positive inotropic action influencing thrombocyte aggregation and improving microcirculation. Hydrazinophenyl heterocyclic intermeidates are also disclosed.

Abstract: The present invention provides indole derivatives of the general formula: ##STR1## wherein R.sub.1 is a hydrogen atom or an alkyl, alkenyl, cycloalkyl, cycloalkenyl, carboxyl, cyano, alkylcarbonyl, alkoxycarbonyl, aminocarbonyl, alkylaminocarbonyl, dialkylaminocarbonyl or aryl radical, R.sub.2 is a hydrogen atom or an alkyl, trihalogenomethyl, hydroxyl, cycloalkyl, cyano, carboxyl, alkoxycarbonyl, alkylcarbonyl, aminocarbonyl, alkylaminocarbonyl or dialkylaminocarbonyl radical; R.sub.2 is a heterocyclic five-membered ring containing 1 to 4 heteroatoms or a heterocyclic six-membered ring containing 1 to 5 heteroatoms, the heteroatoms of the five- and six-membered rings being the same or different and being nitrogen, oxygen or sulphur and one or more of the nitrogen atoms optionally carrying an oxygen atom, the said five- and six-membered rings optionally being substituted by one or more alkyl, alkoxy, alkylthio, oxo, hydroxyl, nitro, amino, halogen or cyano groups; or R.sub.

Abstract: Compounds of the formulas: ##STR1## wherein Het is an oxazole or oxazine moiety; X is O, S or SO, n is an integer from 3 to 9, Y is an aliphatic bridge; and the various R groups represent hydrogen or various substituents as described herein, are useful as antiviral agents, especially against picornaviruses. N-(Chloroalkyl)amide intermediates for the compounds of Formula I are also active as antiviral agents. Related compounds outside the scope of the above formulas are also disclosed.