Abstract: This invention relates to anti-inflammatory compounds, methods of making such compounds and methods of using such compounds having the following structure:

Abstract: A method of modifying or altering the structure of a 1&agr;-hydroxylated vitamin D compound to increase its biological activity by altering the conformational equilibrium of the A-ring to favor a chair conformation that presents the 1&agr;-hydroxyl in the axial orientation. This is accomplished by either locking the A-ring chair conformation in a geometry having an axially orientated 1&agr;-hydroxyl, or by the addition of one or more substituents to the A-ring which interact with other substituents in the molecule or on the A-ring to provide a driving force to the A-ring to adopt a chair conformation which presents the 1&agr;-hydroxyl in the axial orientation.

Abstract: The comprehensive pharmacologic therapy for treatment of obesity is a procedure which involves the administration of a desired therapeutic range of Diethylpropion and/or Phentermine in combination with a SSRI medication and nutritional supplementation for brief and long durations which may be 12 months or more. The preferred procedure involves the administration of drugs in combination which are identified as: Citalopram (Celexa) and Phentermine; Citalopram (Celexa) and Diethylpropion; Citalopram (Celexa), Phentermine, and Diethylpropion. In addition nutritional supplementation such as a multivitamin, 5-Hydroxytryptophan, vitamin B6, vitamin C, Tyrosine, Calcium, and Lysine may be used to enhance the performance of the weight loss treatment program.

Abstract: Described are substituted cyanoenamines of formula I wherein Z, R1, R2 and R3 are defined in the description, compositions thereof and methods for preparing these compounds. These compounds are useful in the treatment of diseases of the central nervous system, the cardiovascular system, the pulmonary system, the gastrointestinal system and the endocrinologic system.

Abstract: Anticonvulsant derivatives useful for preventing the development of Type II diabetes mellitus and Syndrome X are disclosed.

Abstract: Described are substituted cyanoenamines of formula I wherein Z, R1, R2 and R3 are defined in the description, compositions thereof and methods for preparing these compounds. These compounds are useful in the treatment of diseases of the central nervous system, the cardiovascular system, the pulmonary system, the gastrointestinal system and the endocrinologic system.

Abstract: Compounds of formula I activate the insulin receptor kinase. Pharmaceutical compositions comprising the compounds, and methods of treatment of hyperglycemia and other diseases involving imbalance of glucose levels, especially for the treatment of type II diabetes, by administering these compounds to mannnalian hosts, and processes for their preparation, are also described.

Abstract: The invention relates to novel compounds of the formula in which R1 is C1-4alkyl and (Y—X) is CH2, C1-2alkylthio-CH═ or C1-2alkyl-ON═ and Z is an aldimino or ketimino group, and to their preparation, as well as fungicidal compositions with such compounds as active substances. The compounds can be employed for controlling fungi in agriculture, in horticulture and in wood preservation.

Abstract: The invention concerns aryloxypropanolamnine derivatives having at least an anti-diabetic and anti-fat activity and their methods of preparation and applications, particularly as human and veterinary medicine and animal food additive. These derivatives comply with the general formula (I) in which R2 represents one of the following groups: —CH2—, —CH2—CH2, —CH(CH3)—CH2—C(CH3)—CH—, —C(CH3)2—CH2— or a bond; Q represents: (i) a phenyl radical 3,4-substituted alkylene dioxy determining with the phenyl radical, a non-substituted benaodioxane unit, a non-substituted benzodioxol unit, or a 2-substituted benzodioxol unit, (ii) a phenyl radical 3 and/or 4-substituted, by a O—(CH2)x—COOR5 group, (iii) a condensed polycyclic hydrocarbon comprising at least two condensed cycles, (iv) a cyclic hydrocarbon system, optionally cross-linked, and constituting a cycloalkane comprising 1, 2 or 3 cycles.

Abstract: A phytomicrobicidal composition comprising such an amount of at least two active ingredient components that a synergistic effect is achieved, together with a suitable carrier material, wherein component I is a compound of the formula I 1

Abstract: The present invention features compounds able to modulate one or more activities of an inorganic ion receptor and methods for treating diseases or disorders using such compounds. Preferred compounds can mimic or block the effect of extracellular calcium on a cell surface calcium receptor.

Abstract: Compounds of the formula I in which Y is hydrogen, C1-C4alkyl, C1-C4alkoxy, OH, CN, NO2, Si(CH3)3, CF3 or halogen, Z is a group a) R1 is hydrogen, C1-C4alkyl, C2-C4alkenyl, C2-C4alkynyl, C3-C6cycloalkyl, phenyl which is unsubstituted or at most trisubstituted by halogen, C1-C4alkyl, C1-C4alkoxy, C1-C4alkylthio, or benzyl which is unsubstituted or at most trisubstituted in the aromatic ring in the same manner, or is cyclopropylmethyl, C1-C4haloalkyl, C2-C5alkoxyalkyl, cyanomethyl, CO—R6, OH, NH2, C1-C4alkylamine or C1-C4alkoxycarbonyl-C1-C2alkyl; X is oxygen, sulfur or NR5; R2 is hydrogen, C1-C4alkyl, C2-C4alkenyl, C2-C4alkynyl, C3-C6cycloalkyl, C(O)R6, OH or C1-C4alkoxy, NH2 or C1-C4alkylamine; R5 is hydrogen, C1-C4alkyl, C2-C4alkenyl or C2-C4alkynyl; R6 is hydrogen, C114 C4alkyl, C1-C4haloalkyl, C1-C4alkoxy, C3-C6cycloalkyl, C1-C4alkoxycarbonyl or phenyl which is unsubstituted or at most trisubstituted; and in which R3 and R4 independently of one another are hy

Abstract: Compounds related to lactacystin and lactacystin &bgr;-lactone, pharmaceutical compositions containing the compounds, and methods of use.

Abstract: Compounds useful as potassium channel inhibitors and especially useful for the treatment of cardiac arrhythmias and cell proliferative disorders are described.

Abstract: A phytomicrobicidal composition comprising such an amount of at least two active ingredient components that a synergistic effect is achieved, together with a suitable carrier material, wherein component I is a compound of the formula I in which: X is CH or N; R is CH3 or cyclopropyl; Y is H, F, Cl, Br, CF3, CF3O, propargyloxy; Z is H, F, Cl, CF3, CF3O; or Y and Z together are a methylenedioxy, a (difluoromethylene)dioxy, an ethylenedioxy, a (trifluoroethylene)dioxy or a benzo group; and wherein component II is a compound selected from the group consisting of II A) metalaxyl, II B) R-metalaxyl, II C) furalaxyl, II D) benalaxyl, II E) ofurace, II F) oxadixyl, II G) cymoxanil and II H) mancozeb.

Abstract: Compounds represented by formula I: or a pharmaceutically acceptable salt or hydrate thereof, are disclosed. Pharmaceutical compositions and methods of treatment are also included.

Abstract: Selected bis-amino acid hydroxyethylamino sulfonamide compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease. The present invention relates to such retroviral protease inhibitors and, more particularly, relates to selected novel compounds, composition and method for inhibiting retroviral proteases, such as human immunodeficiency virus (HIV) protease, prophylactically preventing retroviral infection or the spread of a retrovirus, and treatment of a retroviral infection.

Abstract: Novel compounds of the general formula: 1

Abstract: The present invention relates to compounds of Formula I that inhibit matrix metalloproteinases and to a method of inhibiting matrix metalloproteinases using the compounds. wherein Q is an un-natural amino acid. More particurlarly, the present invention relates to a method of treating diseases in which matrix metalloproteinases are involved such as multiple sclerosis, atherosclerotic plaque rupture, restenosis, aortic aneurism, heart failure, periodontal disease, corneal ulceration, burns, decubital ulcers, chronic ulcers or wounds, cancer metastasis, tumor angiogenesis, arthiritis, or other autoimmune or inflammatory diseases dependent upon tissue invasion by leukocytes.

Abstract: Pesticidally active cyclohexadienyl derivative compounds of the formula I that are esters, oximes or amides are claimed. These compounds may be used as fungicides, acaricides and insecticides in plant protection.

Abstract: The invention provides compounds, compositions and methods relating to novel electrophilic aromatic derivatives and their use as pharmacologically active agents. The compositions find particular use as pharmacological agents in the treatment of disease states, particularly cancer, psoriasis, vascular restenosis, infections, atherosclerosis and hypercholesterolemia, or as lead compounds for the development of such agents.

Abstract: This invention provides methods of treating secretory diarrhea or cystic fibrosis in a mammal which comprises administering to a mammal in need thereof an effective amount of diarylsulfonylurea. This invention also describes specific diarylsulfonylureas for use in treating secretory diarrhea or cystic fibrosis.

Abstract: This invention provides a method of treating obesity, generalized anxiety disorder, post-traumatic stress disorder, late luteal phase disphoric disorder (premenstrual syndrome), attention deficit disorder, with and without hyperactivity, Gilles de la Tourette syndrome, bulimia nervosa or Shy Drager Syndrome in a mammal by administering to the mammal an effective amount of a hydroxycycloalkanephenethyl amine of the following structural formula: 1

Abstract: The invention relates to compounds of the formula in which: A is a divalent radical selected from: A1) —O—CO— A2) —CH2—O—CO— A3) —O—CH2—CO— A4) —O—CH2—CH2— A5) —N(R1)—CO— A6) —N(R1)—CO—CO— A7) —N(R1)—CH2—CH2— A8) —O—CH2— in which: R1 is a hydrogen or a (C1-C4)-alkyl; and Am is a nitrogen-containing heterocycle.

Abstract: The present invention relates to dioxocyclopentyl hydroxamide derivatives of the formula wherein X, Z and Q are as defined in the specification, and to pharmaceutical compositions and methods of treatment thereof.

Abstract: Compounds of the formula I in which Y is hydrogen, C1-C4alkyl, C1-C4alkoxy, OH, CN, NO2, Si(CH3)3, CF3 or halogen, Z is a group a) R1 is hydrogen, C1-C4alkyl, C2-C4alkenyl, C2-C4-alkynyl, C3-C6cycloalkyl, phenyl which is unsubstituted or at most trisubstituted by halogen, C1-C4alkyl, C1-C4alkoxy, C1-C4alkylthio, or benzyl which is unsubstituted or at most trisubstituted in the aromatic ring in the same manner; or is cyclopropylmethyl, C1-C4haloalkyl, C2-C5alkoxyalkyl, cyanomethyl, CO—R6, OH, NH2, C1-C4alkylamine or C1-C4alkoxycarbonyl-C1-C2alkyl; X is oxygen, sulfur or NR5; R2 is hydrogen, C1-C4alkyl, C2-C4alkenyl, C2-C4alkynyl, C3-C6cycloalkyl, C(O)R6, OH or C1-C4alkoxy, NH2 or C1-C4alkylamine; R5 is hydrogen, C1-C4alkyl, C2-C4alkenyl or C2-C4alkynyl; R6 is hydrogen, C114 C4alkyl, C1-C4haloalkyl, C1-C4alkoxy, C3-C6cycloalkyl, C1-C4alkoxycarbonyl or phenyl which is unsubstituted or at most trisubstituted; and in which R3 and R4 independently of one another are h

Abstract: A compound of formula (I), in which: R1 is lower alkyl, cyclo(lower)alkyl, optionally substituted aryl, optionally substituted heterocyclic group, cyclo(lower)alkyl(lower)alkyl, or ar(lower)alkyl; R2 is hydrogen, hydroxy or protected hydroxy; R3 is lower alkyl, aryl, ar(lower)alkyl or optionally substituted heterocyclic(lower)alkyl; R4 is carboxy, protected carboxy or lower alkylsufonylcarbamoyl; R5 is hydrogen or lower alkyl; R6 is hydrogen or heterocyclic group; A is a single bond or lower alkylene, and Ar is optionally substituted aryl, or pharmaceutically acceptable salts thereof, having endothelin antagonistic activity.

Abstract: A method for the inhibition of the binding of &agr;4&bgr;1 integrin to its receptors, for example VCAM-1 (vascular cell adhesion molecule-1) and fibronectin; compounds that inhibit this binding; pharmaceutically active compositions comprising such compounds; and the use of such compounds either as above, or in formulations for the control or prevention of diseases states in which &agr;4&bgr;1 is involved.

Abstract: The present invention provides non-peptide cathepsin D binding compounds and methods for using such compounds in the detection, labelling and inhibition of cathepsin D.

Abstract: A compound of formula (i) ##STR1## has therapeutic utility via inhibition of phosphodiesterase and THF release.

Abstract: This invention is directed to compounds of formula I ##STR1## wherein R.sup.1 is CN, CH.sub.2 CN, CH.dbd.CHCN, CHO, or CH.dbd.CHCO.sub.2 H;R.sup.2 is aryl lower alkoxy, heteroaryl lower alkoxy, aryl lower alkylthio or heteroaryl lower alkylthio wherein each of the aryl and heteroaryl moieties is optionally substituted;R.sup.3 is halogen;R.sup.4 is optionally substituted aryl or optionally substituted heteroaryl;R.sup.5 is carboxy or an acid isostere;X is oxygen or sulphur; andn is zero or 1; or an N-oxide thereof, prodrug thereof solvate thereof, or pharmaceutically acceptable salt thereof, which compounds have endothelin antagonist activity. The invention is also directed to methods for preparing the compounds of formula I and their pharmaceutical use.

Abstract: The present invention relates to methods and pharmaceutical compositions for stimulating the growth of neurites in nerve cells. The compositions comprise a neurotrophic amount of a compound which binds to the FK-506 binding protein (FKBP) and a neurotrophic factor, such as nerve growth factor NGF. The methods comprise treating nerve cells with the above-described compositions or compositions comprising the FKBP binding compound without a neurotrophic factor. The methods of this invention can be used to promote repair of neuronal damage caused by disease or physical trauma.

Abstract: This invention relates to insecticidal compositions comprising one or more substituted N,N'-dibenzoyl-N'-tert-alkyl-hydrazines and diethyl maleate which exhibit improved activity as insecticides when compared to compositions without diethylmaleate.

Abstract: Novel nonpeptide antagonists of endothelin I are described, as well as methods for the preparation and pharmaceutical compositions of the same, which are useful in treating elevated levels of endothelin, acute and chronic renal failure, hypertension, myocardial infarction, myocardial ischemia, cerebral vasospasm, cerebral ischemia, cerebral infarction, cirrhosis, septic shock, congestive heart failure, endotoxic shock, subarachnoid hemorrhage, arrhythmias, asthma, preeclampsia, atherosclerotic disorders including Raynaud's disease and restenosis, angina, cancer, pulmonary hypertension, ischemic disease, gastric mucosal damage, hemorrhagic shock, ischemic bowel disease, stroke, benign prosthatic hyperplasia (BPH), and diabetes.

Abstract: This invention relates to N'-substituted-N,N'-disubstitutedhydrazines of formula I ##STR1## wherein X and X' are independently O, S, or NR; A' and B' are independently substituted or unsubstituted aryl or aromatic heterocycle; wherein F is alkyl, alkenyl, or aralkyl; and wherein E is a tertiary carbon containing organic radical having a total of at least four carbon and halogen atoms but not more than six halogen atoms, or a non-tertiary carbon containing non-haloalkyl organic or organometallic radical having at least five atoms other than hydrogen, oxygen and halogen which are useful as insecticides, compositions containing those compounds, methods of producing the compounds, and methods of their use. More particularly, the invention relates to insect growth regulating compounds and compositions, and methods of using such compounds and compositions. Compounds of the present invention are particularly suitable for controlling plant-destructive insects in crops of cultivated plants, ornamentals and forestry.

Abstract: Compounds of the formula I or II ##STR1## are suitable for the production of pharmaceuticals for the modulation of apoptosis. These compounds can be employed for the treatment of infarct, stroke, neurodegeneration or hypertrophic disorders.

Abstract: Carboxylic acid derivatives of the formula I ##STR1## here R.sup.1 is a tetrazole [sic], nitrile [sic], a group COOH or a radical which can be hydrolyzed to COOH, and the other substituents have the meaning explained in the description.

Abstract: Novel derivatives of benzodioxa alkylene ethers are provided which are useful as melatonergic agents.

Abstract: A compound represented by general formula (I) or a pharmaceutically acceptable salt or ester thereof: [wherein each of Ar.sup.1, Ar.sup.2, Ar.sup.3 and Ar.sup.4 is an aryl group or an aromatic heterocyclic group; A.sup.1 is a C.sub.2-6 chain hydrocarbon group or a group represented by --A.sup.1a --W.sup.1 --A.sup.1b -- (wherein W.sup.1 is an oxygen atom, a sulfur atom, an ethynylene group, a cyclopropylene group or a group represented by --NR.sup.W --; A.sup.2 is a C.sub.2-8 chain hydrocarbon group; each of X and Y is an oxygen atom, a sulfur atom, a carbonyl group or a group represented by --CHR.sup.a -- or by --NR.sup.b --, or X and Y together represent a vinylene group or an ethynylene group; each of R.sup.1, R.sup.2, R.sup.3, R.sup.7 and R.sup.8 is a hydrogen atom, a halogen atom, a hydroxyl group, a lower alkyl group, a lower alkenyl group or a lower alkoxy group; each of R.sup.4 and R.sup.

Abstract: A phenylacetamide derivative of formula (I) have potent analgesic and anti-inflammatory activities and exhibit less irritability and toxicity: ##STR1## wherein, X, Y, W, n, m and Ar are as defined in the specification.

Abstract: .alpha.- and .beta.-amino acid hydroxyethylamino sulfonamide compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease.

Abstract: FK506 and geldanamycin promote nerve regeneration by a common mechanism that involves the binding of these compounds to polypeptide components of steroid receptor complexes other than the steroid hormone binding portion of the complex (FKBP52 and hsp90, respectively). These and other agents cause hsp90 dissociation from steroid receptor complexes or block association of hsp90 with steroid receptor complexes.

Abstract: The present invention provides dihalopropene compounds of the general formula: ##STR1## wherein R.sub.1 is C.sub.1 -C.sub.10 alkyl or the like; L is C(.dbd.O)NH or the like; R.sub.2, R.sub.3 and R.sub.4 are independently halogen or the like; R.sub.5, R.sub.6 and R.sub.7 are independently hydrogen or the like; m is an integer of 0 to 4; n is an integer of 0 to 2; X is chlorine or the like; Y is oxygen or the like; and Z is oxygen or the like, which have excellent insecticidal activity so that they are satisfactorily effective for the control of noxious insects.

Abstract: This invention relates to novel statone antiviral analogs, to the processes and intermediates useful for their preparation and to their use as antiviral agents.

Abstract: Amino acid derivatives of formula (Ia) and (Ib) and pro-drugs thereof containing a group responsible for chelating the zinc atom of enkephalinase and angiotensin convertase enzymes are disclosed as inhibitors of these enzymes.

Abstract: Imide compounds having a propioloyl group or pharmaceutically acceptable salts thereof which exhibit potent activities to inhibit the production of Interleukin 1-.beta. and also the production of Tumor Necrosis Factor .alpha.. These imide compounds are useful as a prophylactic or therapeutic agent for inhibiting the production of Interleukin 1-.beta. and the production of Tumor Necrosis Factor .alpha., typically for such diseases as chronic rheumatism, sepsis, ulcerative colitis, Crohn's disease and many other related diseases in which Interleukin 1-.beta. and/or Tumor Necrosis Factor .alpha. would participate.

Abstract: The present invention relates to difluorostatone derivatives useful as antiviral agents.

Abstract: Compounds of the formula ##STR1## wherein the variables are defined as in the specification, are capable of lowering introaocular pressure in the eye of a mammal.

Abstract: This invention relates to the method of using specially formulated neurotrophic pipecolic acid derivative compounds having an affinity for FKBP-type immunophilins as inhibitors of the enzyme activity associated with immunophilin proteins, and particularly inhibitors of peptidyl-prolyl isomerase or rotamase enzyme activity to stimulate or promote neuronal growth or regeneration.

Abstract: The present invention provides an antibacterial and fungicidal agent containing an amino compound of formula (1) or a salt thereof. The invention also provides a method for imparting antibacterial and fungicidal properties to a variety of objects using the compound. ##STR1## wherein .phi. represents a phenyl group, a substituted phenyl group (wherein the substituents are 1-5 members arbitrarily selected from the group consisting of a hydroxyl group, halogen atoms, lower alkoxyl groups, trifluoromethyl group, an amino group, and a methylenedioxy group), or an imidazolyl group; R.sup.1 represents a hydrogen atom or a lower alkyl group; and R.sup.2 represents a C6-C12 alkyl group. The amino compound of formula (1) or a salt thereof exhibits excellent antibacterial effects and fungicidal effects, and when it is applied to a variety of articles used in industry, commodities, etc., enhanced antibacterial effects and fungicidal effects are obtained.