Abstract: The present invention provides a process for the preparation of crude 1-[3-(dimethylamino)propyl]-1-(4-fluorophenyl)-1,3-dihydro-5-isobenzofuran carbonitrile base with substantially low levels of impurities by arresting the formation of substantial amount of carboxamide impurity, high molecular weight impurities and suppressing the formation of desmethylcitalopram besides taking the cyanide exchange reaction to near completion and thus avoiding an extensive and expensive purification process.

Abstract: A process for the preparation of prostaglandin compounds having the formula (I): wherein A is selected from the group consisting of C1–C6 alkyl groups; C7–C16 aralkyl groups wherein an aryl portion thereof is unsubstituted or substituted with one to three substituents selected from the group consisting of C1–C6 alkyl groups, halo and CF3; and (CH2)nOR? wherein n is an integer from 1 to 3 and R? represents a C6–C10 aryl group which is unsubstituted or substituted with one to three substituents selected from the group consisting of C1–C6 alkyl groups, halo and CF3; B is selected from OR? and NHR? wherein R? is C1–C6 alkyl groups; and represents a double bond or a single bond, is disclosed. Novel intermediates are also disclosed.

Abstract: The invention relates to anthranilic acid amides and the use thereof as medicaments for the treatment of diseases that are triggered by persistent angiogenesis, in addition to intermediate products in the production of anthranilic acid amides.

Abstract: A process for the preparation of prostaglandin compounds having the formula (I): wherein A is selected from the group consisting of C1–C6 alkyl groups; C7–C16 aralkyl groups wherein an aryl portion thereof is unsubstituted or substituted with one to three substituents selected from the group consisting of C1–C6 alkyl groups, halo and CF3; and (CH2)nOR? wherein n is an integer from 1 to 3 and R? represents a C6–C10 aryl group which is unsubstituted or substituted with one to three substituents selected from the group consisting of C1–C6 alkyl groups, halo and CF3; B is selected from OR? and NHR? wherein R? is C1–C6 alkyl groups; and represents a double bond or a single bond, is disclosed. Novel intermediates are also disclosed.

Abstract: The present invention provides novel compounds, compositions containing the compounds of the invention in a pharmaceutically acceptable excipient and methods for using the compositions for lowering intraocular pressure.

Abstract: Chemical compounds which are antagonists of Monocyte Chemoattractant Protein-1 (MCP-1) function, pharmaceutical compositions comprising these compounds, methods of treatment employing these compounds and compositions, and processes for preparing these compounds. The compounds are useful in the prevention or treatment of chronic or acute inflammatory or autoimmune diseases, especially those associated with aberrant lymphocyte or monocyte accumulation such as arthritis, asthma, atherosclerosis, diabetic nephropathy, inflammatory bowel disease, Crohn's disease, multiple sclerosis, nephritis, pancreatitis, pulmonary fibrosis, psoriasis, restenosis, and transplant rejection.

Abstract: Insecticidal (dihalopropenyl) phenylalkyl substituted dihydrobenzofuran and dihydrobenzopyran derivatives of Formula I are disclosed. These compounds provide unexpected insecticidal activity across a spectrum of insect pests combined with desirable physical properties including improved photostability. wherein x and y are integers independently selected from 0 or 1; and B is a bridging group *—(CR16R17)q—(CR18R19)r—(CR20R21)s—Lt—(CR22R23)u—(CR24R25)v—(CR26R27)w—, where the asterisk denotes attachment at A; and q, r, s, u, v and w are integers independently selected from 0, 1 and 2; and t is an integer selected from 0 and 1. A, D, E, G, M, R through R11, and R16 through R27, inclusively, are fully described herein. In addition, compositions comprising an insecticidally effective amount of at least one compound of formula I and methods of controlling insects by applying said compositions to a locus where insects are present or are expected to be present are also disclosed.

Abstract: The invention relates to benzofuran or benzothiophene derivatives, to processes for preparing them, to pharmaceutical compositions comprising them, and to the method of use thereof in the treatment of pathological syndromes of the cardiovascular system.

Abstract: New compounds represented by the formula or pharmaceutically acceptable salts or prodrugs thereof, wherein X1 and X2 are each independently selected from a CH group or a nitrogen atom; and R is an optionally substituted five or six membered nonaromatic carbocyclic ring or a nonaromatic or aromatic heterocyclic ring, whereby the ring is optionally condensed with a 6-membered, optionally substituted carbocyclic aromatic ring.

Abstract: A stable solid hydrate of a muscarinic receptor antagonist is useful in the treatment of irritable bowel syndrome, diverticular disease, oesophageal achalasia, chronic obstructive airways disease, over active bladder (including symptoms of incontinence, urge and frequency), urinary incontinence, neurogenic urinary urgency or pollakiuria, treatment of bladder functional disorder, urinary leakage, painful or difficult urination caused by neurogenic bladder, spastic or hypertonic bladder, dysfunctional bladder syndrome, gastrointestinal disorders including gastrointestinal hyperactivity, and relaxing effect on intestinal smooth muscle cells.

Abstract: A sulfonamide compound of the formula (I): R1—SO2NHCO—A—X—R2??(I) wherein R1 is alky, alkenyl, alkynyl and the like; A is an optionally substitutedheteropolycyclic group except benzimidazolyl, indolyl, 4,7-dihydrobenzimidazolyland 2,3-dihydrobenzoxazinyl; X is alkylene, oxa, oxa(lower)alkylene and the like; and R2 is optionally substituted aryl, substituted biphenylyl and the like, a salt thereof and a pharmaceutical composition comprising the same. The sulfonamide compound is effective for the diseases treatable based on their blood sugar level-depressing activity, cGMP-PDE (especially PDE-V)-inhibiting activity, smooth muscle relaxing activity, bronchodilating activity, vasodilating activity, smooth muscle cell suppressing activity, and antiallergic activity.

Abstract: This invention relates to compounds which are generally IP receptor antagonists and which are represented by Formula I: wherein G1 is selected from the group consisting of a, b1 and b2, and A and G2 are as defined in the specification; or pharmaceutically acceptable salts or solvates thereof. The invention further relates to pharmaceutical compositions containing such compounds, methods for their use as therapeutic agents, and methods of preparation thereof.

Abstract: The present invention relates to compounds of the formula I in which one of the radicals R8 and R9 is a hydrogen atom or an alkyl group and the other is hydroxyl, alkoxy or acyloxy or where R8 and R9, together with the carbon atom to which they are bonded, are a carbonyl group and the radicals R1 to R7 have the meanings indicated in the description. The compounds inhibit the release of various mediators of the arachidonic acid cascade and can thus be used for the prevention of allergically induced disorders or for the treatment of disorders of the rheumatic type.

Abstract: New compounds represented by the formula or pharmaceutically acceptable salts or prodrugs thereof, wherein X1 and X2 are each independently selected from a CH group or a nitrogen atom; and R is an optionally substituted five or six membered nonaromatic carbocyclic ring or a nonaromatic or aromatic heterocyclic ring, whereby the ring is optionally condensed with a 6-membered, optionally substituted carbocyclic aromatic ring.

Abstract: The present invention relates to compounds of the general formula (I) The compounds are useful in the treatment and/or prevention of conditions mediated by nuclear receptors, in particular the Peroxisome Proliferator-Activated Receptors (PPAR).

Abstract: The present invention relates to a novel process for the nitration of organic compounds, preferably of aromatic and heteroaromatic compounds, using nitrating reagents which are known from the literature and new types of nitrating reagents.

Abstract: An industrially useful process for producing benzofuran derivatives of formula (1): by formylating a compound of formula (2): (where A1 is a protective group), followed by reaction with a compound of formula (4): (where X1 is a halogen atom), then performing a cyclizing reaction and subsequently performing a reaction for hydroxyl group deprotection.

Abstract: The invention relates to 2-butyl-5-(methanesulfonamido)benzofuran, its preparation and its use. This compound is a synthesis intermediate, in particular for the preparation of dronedarone.

Abstract: Bi-aromatic compounds linked via a heteroethynylene radical are provided along with pharmaceutical and cosmetic compositions containing these compounds and methods for their use.

Abstract: A process for preparing heterocyclic pentalene derivative having formula (I): wherein w is a sulfur atom (S), an oxygen atom (O) or a NR or PR group, wherein R is an hydrocarbon group; R1, R2, R3, and R4, equal to or different from each other, are hydrogen atoms or hydrocarbon groups; said process comprising the following steps: a) contacting a compound of formula (II) T is a OR, NR2, CCI3, CF3, Cl, Br, I, imidazolil or pirazolyl radical; with at least one molar equivalent of a vinyl compound of formula (III): wherein M is MgHal, Li, K, ZnHal, wherein Hal is chlorine, bromine or iodine; (II), (III) b) treating the compound of formula obtained in step a) with a Bronsted acid; c) treating the compound obtained in step b) with a reducing agent; and d) dehydrating the alcohol obtained in step c) in order to obtain the compound of formula (I).

Abstract: A sulfonamide compound of the formula (I): R1—SO2NHCO—A—X—R2  (I) wherein R1 is alky, alkenyl, alkynyl and the like; A is an optionally substitutedheteropolycyclic group except benzimidazolyl, indolyl, 4,7-dihydrobenzimidazolyland 2,3-dihydrobenzoxazinyl; X is alkylene, oxa, oxa(lower)alkylene and the like; and R2 is optionally substituted aryl, substituted biphenylyl and the like, a salt thereof and a pharmaceutical composition comprising the same. The sulfonamide compound is effective for the diseases treatable based on their blood sugar level-depressing activity, cGMP-PDE (especially PDE-V)-inhibiting activity, smooth muscle relaxing activity, bronchodilating activity, vasodilating activity, smooth muscle cell suppressing activity, and antiallergic activity.

Abstract: This invention relates to a series of substituted aromatic ethers of the formula I wherein ring A and X and Y are defined as in the specification, that exhibit activity as glycine transport inhibitors, their pharmaceutically acceptable salts, pharmaceutical compositions containing them, and their use for the enhancement of cognition and the treatment of the positive and negative symptoms of schizophrenia and other psychoses in mammals, including humans.

Abstract: A process for the preparation heterocyclic indene analogs, especially with the preparation of 4-hydroxycarbazole or N-protected 4-hydroxycarbazole, involves cyclocarbonylation followed by saponification. This process avoids high temperatures and high catalyst loadings.

Abstract: Compounds of the general formula (I): 1

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: A compound having a partial structure represented by Formula: 1

Abstract: Nobel PDF inhibitors and novel methods for their use are provided.

Abstract: PDE4 inhibition is achieved by novel compounds, e.g., aminoindazole and aminobenzofuran analogs.

Abstract: A process for preparing optically active 2,3-dihydrobenzofuran compounds which comprises subjecting a 2,3-dihydrobenzofuran compound represented by the general formula or a salt thereof to optical resolution with an optically active acid compound: 1

Abstract: Bicyclic cyclopropane derivatives of the general Formula (I) 1

Abstract: A process for removing acids from reaction mixtures using an auxiliary base, in which the auxiliary base

Abstract: Compounds of the formula where the variables have the meaning defined in the specification, are specific or selective agonists of RXR retinoid receptors.

Abstract: An oxygen-containing heterocyclic compound represented by following Formula (I): wherein R1 and R2 independently represent hydrogen, lower alkyl, cyano, —(CH2)n—E1—CO—G1 (wherein E1 represents a bond, O, or NH; and G1 represents hydrogen, substituted or unsubstituted lower alkyl, OR6, or NR7R8; and n represents an integer of 0 to 4), or the like; R1 and R2 are combined to represent a saturated carbon ring together with a carbon atom adjacent thereto; or R2, and R11 or R13 described below are combined to form a single bond; R3 represents hydrogen, phenyl, or halogen; R4 represents hydroxy, lower alkoxy, or the like; A represents —C(R9)(R10)— or O; B represents O, NR11, —C(R12)(R13)—, or —C(R14)(R15)— C(R16)(R17)—; D represents (i) —C(R18)(R19)—X— (wherein X represents —C(R21)(R22)—, S, or NR23), (ii) —C(R19a)═Y— [Y represents —C(R24)—Z— (wherein Z represents

Abstract: Certain benzofuran derivatives are useful in the treatment of certain ischemic or inflammatory conditions, as well as neuroinflammation, neurodegeneration or degenerative diseases in which mitochondrial dysfunction leads to tissue degeneration. They are also useful in the manufacture of pharmaceutical formulations for the treatment of such conditions.

Abstract: The invention describes novel substituted aryl compounds that are cyclooxygenase 2 (COX-2) selective inhibitors and novel compositions comprising at least one cyclooxygenase 2 (COX-2) selective inhibitor, and, optionally, at least one compound that donates, transfers or releases nitric oxide, stimulates endogenous synthesis of nitric oxide, elevates endogenous levels of endothelium-derived relaxing factor or is a substrate for nitric oxide synthase, and/or, optionally, at least one therapeutic agent, such as, steroids, nonsterodal antiinflammatory compounds (NSAID), 5-lipoxygenase (5-LO) inhibitors, leukotriene B4 (LTB4) receptor antagonists, leukotriene A4 (LTA4) hydrolase inhibitors, 5-HT agonists, 3-hydroxy-3-methylglutaryl coenzyme A (HMG-CoA) inhibitors, H2 antagonists, antineoplastic agents, antiplatelet agents, thrombin inhibitors, thromboxane inhibitors, decongestants, diuretics, sedating or non-sedating anti-histamines, inducible nitric oxide synthase inhibitors, opioids, analgesics, Helicobacter pyl

Abstract: There is described a process for the preparation of 5-carboxy phthalide, which comprises adding terephthalic acid to fuming sulfuric acid containing at least 20% of SO3, then adding formaldehyde to the mixture, heating the mixture at a temperature of 120-145° C. and isolating 5-carboxyphthalide from the reaction mixture.

Abstract: A diverse set of tubulin binding agents have been discovered which are structurally characterized, in a general sense, by a semi-rigid molecular framework capable of maintaining aryl-aryl, pseudo pi stacking distances appropriate for molecular recognition of tubulin. In phenolic or amino form, these ligands may be further functionalized to prepare phosphate esters, phosphate salts, phosphoramidates, and other prodrugs capable of demonstrating selective targeting and destruction of tumor cell vasculature.

Abstract: The present invention provides a production method of a 5-phthalancarbonitrile compound, which comprises the use of a novel compound of the formula [I] 1

Abstract: A compound of formula (I): wherein: R1 represents hydrogen, halogen, alkyl or alkoxy, X represents oxygen, sulphur or NR wherein R represents hydrogen or alkyl, A represents any one of the groups described in the description, their isomers and addition salts thereof with a pharmaceutically acceptable acid or base and medicinal products containing the same are useful as metalloprotease inhibitor.

Abstract: The invention relates to an optically active isosorbide derivative represented by general formula (I) and an optically active isomannide derivative represented by general formula (V), General formula (I) 1

Abstract: The present invention relates to the novel isolated 12-30 strain of Pestalotiopsis microspora capable of producing novel antioxidant and antimycotic agents. The present invention also relates to the novel isolated 3,5,7 trisubstituted isobenzofuranone and derivatives thereof, methods of isolating the novel isobenzofuranone from cultures P. microspora 12-30, and to novel uses of the compound as an antioxidant and antimycotic agent. The present invention further relates to a novel 1,5,7 trisubstituted 1,3-dihydroisobenzofuran and derivatives thereof, methods of isolating this novel compound from cultures of Pestalotiopsis microspora 12-30, and to uses thereof.

Abstract: A class of compounds is described which can be used for the treatment of viral infections. Compounds of particular interest are defined by Formula II wherein each of R1, R2, and R3 is independently selected from hydrido, halo, and nitro; wherein R8 is selected from haloalkyl, optionally substituted aryl, optionally substituted aralkyl, optionally substituted heteroaryl, optionally substituted arylalkoxy and optionally substituted aryloxyalkyl; where Y is selected from fluoroalkyl, and wherein R9 alkylamino; or a pharmaceutically-acceptable salt or tautomer thereof.

Abstract: This invention relates to a series of substituted aromatic ethers of the formula I 1

Abstract: An industrially useful process for producing benzofuran derivatives of formula (1) 1

Abstract: The invention relates to novel (aminoalkenyl-benzoyl) benzofuran or benzothiophene derivatives of general formula: 1

Abstract: Novel processes and intermediates useful in the preparation of 11-oxa prostaglandin analogs are disclosed.

Abstract: A compound of the formula (I): wherein X is hydroxy, protected hydroxy or optionally substituted amino; Y is —COORA wherein RA is hydrogen or ester residue, —CONRBRC wherein RB and RC each is independently hydrogen or amide residue, optionally substituted aryl or optionally substituted heteroaryl; and A1 is optionally substituted heteroaryl; provided that a compound wherein Y and/or A1 is optionally substituted indol-3-yl is excluded, a tautomer, a prodrug, a pharmaceutically acceptable salt or a hydrate thereof has an inhibitory activity against an integrase.

Abstract: This invention relates generally to phosphate esters of bis-amino acid sulfonamides containing substituted benzyl amines of formula I: or stereoisomeric forms, stereoisomeric mixtures, or pharmaceutically acceptable salt forms thereof, which are useful as HIV protease inhibitors, pharmaceutical compositions comprising the same, and methods of using the same for treating viral infection.

Abstract: The invention relates to a method for the 1,3 dipolar cycloaddition of organic compounds, characterised in that the reaction is carried out in a microreactor.

Abstract: The invention concerns compounds of formula (I): R—A—R′ wherein: A is as defined in the description; R represents a group (V), (VI), (VII) or (VIII), where E, Q, R1, R2, R3, v and R4 are as defined in the description; R′ represents a —(CH2)t—R5 group wherein t and R5 are as defined in the description