Abstract: The invention relates to a process for the manufacture of bidentate ligands of the formula IA and IIA, characterized in that N,N-(optionally substituted) dialkylamino phosphines bound to an aromatic carbon are lithiated in ortho-position and the lithiated compounds are further converted to said bidentate ligands: wherein X1 is NR, O or S; X2 is CHR1 or CR1; X3 is CHR2 or NR2 or, if X2 is CR1, X3 is CR2 or N; and R, R1 and R2 are radicals such as alkyl groups or R1 and R2 together form an annealed ring; Y1*, Y2* and Y1?* are, independently of each other, an element of the fifth group of the periodic table of elements as such or in thioxo or oxo form; Z1*, Z2*, Z3*, Z4*, Z1?*, Z2?* are, independently of each other, for example halogen, hydrogen, or an unsubstituted or substituted moiety selected from radicals such as alkyl groups; the substituents have otherwise the meanings given in the specification; and the ligands are capable of forming metal complexes, which can be used as catalysts in stereoselective

Abstract: An imidazoline compound comprising the reaction product of (i) a dicarbonyl, (ii) a primary amine moiety of a polyamine, and (iii) a hydrocarbyl carbonyl is disclosed. Lubricant and fuel additive compositions comprising the imidazoline compound are also disclosed.

Abstract: Tertiary amine compounds that bind chemokine receptors such as CXCR4 and CCR5 are disclosed.

Abstract: The present invention relates to agents for coloring keratin fibers which comprise at least one zwitterionic azo dye of the general formula (I) where R1 is an alkylsulfonate radical of the formula (II),

Abstract: A compound is disclosed herein comprising or a pharmaceutically acceptable salt or a prodrug thereof; wherein R is OH or NH2. Methods, compositions, and medicaments related thereto are also disclosed.

Abstract: The present invention relates to methods for the prophylaxis, management and treatment of certain diseases modulated by the inhibition of the enzyme malonyl-coenzyme A decarboxylase (malonyl-CoA decarboxylase, MCD) by the administration of a composition containing as an active ingredient a compound according to Formula I. In particular, the invention relates to methods for the prophylaxis, management and treatment of cardiovascular diseases, diabetes, acidosis, cancers, and obesity through the administration of a compound which inhibits malonyl-coenzyme A decarboxylase activity.

Abstract: The present invention is concerned with compounds of formula the N-oxides, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein R1 is hydrogen, hydroxy, C1-6alkyl or aryl; R2 is hydrogen; optionally substituted C1-12alkyl; C3-7cycloalkyl; C2-8alkenyl, optionally substituted pyrrolidinyl or aryl; R3 is hydrogen, optionally substituted C1-6alkyl or aryl; Het is an optionally substituted unsaturated heterocycle selected from imidazolyl, triazolyl, tetrazolyl and pyridinyl; is an optionally substituted unsaturated mono- or bicyclic heterocycle; and aryl is optionally substituted phenyl. The present invention also relates to processes for their preparation and compositions comprising said new compounds, as well as their use as a medicine.

Abstract: The invention relates to compounds, compositions comprising the compounds, and methods of using the compounds and compound compositions. The compounds, compositions, and methods described herein can be used for the therapeutic modulation of ion channel function, and treatment of disease and disease symptoms, particularly those mediated by certain calcium channel subtype targets.

Abstract: There is provided a compound of Formula I wherein each T is independently selected from H, hydrocarbyl, —F—R, and a bond with one of D, E, P or Q, or together with one of P and Q forms a ring; Z is a suitable atom the valency of which is m; D, E and F are each independently of each other an optional linker group, wherein when Z is nitrogen E is other than CH2 and C?O; P, Q and R are independently of each other a ring system; and at least Q comprises a sulphamate group.

Abstract: Halogenated carboxylic ester derivatives of phenylethyl imidazole, and their method of preparation are disclosed. Radio-halogenated forms of these compounds are ideally suited for positron-imaging of the adrenal glands, as it is known that these compounds demonstrate a selective and high rate of accumulation in the adrenals. The method of preparing these derivatives proceeds by the conversion of a stable, non-radioactive intermediate having trialkylstannyl leaving groups. These intermediates are efficiently converted to the corresponding halogenated forms by substitution of the trialkylstannyl group with the halogen or radiohalogen.

Abstract: A compound of the formula or a pharmaceutically acceptable salt thereof, is disclosed herein. Methods and compositions related thereto are also disclosed.

Abstract: The present disclosure relates to symmetrical cationic diazo compounds of formula (I) below, their resonance forms, and also their acid addition salts and their solvates: wherein W1 radicals, which are identical, are chosen from a halogen atom, or an —NR4-Ph-NR5R6, —NR4-Ph-OR7, —O-Ph-OR7 or —O-Ph-NR5R6 group or else an —NR5R6 or —OR7 group with certain provisos; L, a non-cationic linker connecting the two identical azo chromophores, is chosen from a covalent bond; an optionally substituted C1-C40 alkyl radical optionally interrupted by a (hetero)cycle, the alkyl radical being optionally interrupted by at least one heteroatom or group comprising at least one heteroatom or an optionally substituted phenyl radical. The disclosure further relates to dyeing compositions comprising such compounds as a direct dye in a medium appropriate for the dyeing of keratin fibers, and also to a method of coloring keratin fibers that employs this composition, and a device comprising a plurality of compartments.

Abstract: Novel phenyltetrazole compounds useful as intermediates in the preparation of angiotensin II antagonists and the processes for the conversion thereof to biologically active molecules.

Abstract: Compounds of Formula 1 where X is S and the variables have the meaning defined in the specification are specific or selective to alpha2B and/or alpha2C adrenergic receptors in preference over alpha2A adrenergic receptors, and as such have no or only minimal cardivascular and/or sedatory activity. These compounds of Formula 1 are useful as medicaments in mammals, including humans, for treatment of diseases and or alleviations of conditions which are responsive to treatment by agonists of alpha2B adrenergic receptors. Compounds of Formula 1 where X is O also have the advantageous property that they have no or only minimal cardivascular and/or sedatory activity and are useful for treating pain and other conditions with no or only minimal cardivascular and/or sedatory activity.

Abstract: The present invention relates to the use of compounds of the general Formula (I): wherein in Formula (I), R is H, alkyl, cycloalkyl, aryl or heteroaryl; R1 is H, alkyl, cycloalkyl, aryl or heteroaryl; R2 is H, alkyl, cycloalkyl, aryl or heteroaryl; A1 and A2 each independently represent an optionally substituted C1-C20-alkyl group which may contain one or more group(s) Z, or a monocyclic or polycyclic optionally substituted aromatic or non-aromatic ring system which may contain one or more group(s) X, and in case of a polycyclic ring system, said system contains at least one aromatic ring; Z is selected from the group consisting of S, O, N, NR4, CO, CO2, CS, SO or SO2 X is selected from the group consisting of S, O, N, NR4, SO or SO2.

Abstract: Aminomethyl substituted tetracycline compounds, pharmaceutical compositions, and methods of use thereof are discussed.

Abstract: The invention relates to R-(?)-1-[2-(7-Chloro-benzo[b]thiophen-3-yl-methoxy)-2-(2,4-dichloro-phenyl)-ethyl]-1H-imidazole and the salts thereof. The invention also relates to compositions thereof and their use either for treating fungal infections in humans and animals or combating crop diseases. A process for their preparation is also described.

Abstract: Compounds of Formula 1 where X is S and the variables have the meaning defined in the specification are specific or selective to alpha2B and/or alpha2C adrenergic receptors in preference over alpha2A adrenergic receptors, and as such have no or only minimal cardivascular and/or sedatory activity. These compounds of Formula 1 are useful as medicaments in mammals, including humans, for treatment of diseases and or alleviations of conditions which are responsive to treatment by agonists of alpha2B adrenergic receptors. Compounds of Formula 1 where X is O also have the advantageous property that they have no or only minimal cardivascular and/or sedatory activity and are useful for treating pain and other conditions with no or only minimal cardivascular and/or sedatory activity.

Abstract: An electroluminescent element is disclosed, comprising an electroluminescent material and a fluorescent substance emitting light having an emission maximum at the wavelength different from that of light emitted from the electroluminescent material upon absorption of the light emitted from the electroluminescent material. A color conversion filter is also disclosed, comprising a fluorescent substance emitting light having an emission maximum at the wavelengths of 400 to 700 nm upon absorption of the light emitted from the electroluminescent material.

Abstract: The present invention provides imidazolyl inhibitors of 15-LO, pharmaceutical compositions containing such inhibitors and methods for treating diseases related to the 15-LO cascade using such compounds and compositions.

Abstract: The present invention relates to dihydropyrazole compounds that are useful for treating cellular proliferative diseases, for treating disorders associated with KSP kinesin activity, and for inhibiting KSP kinesin. The invention also related to compositions which comprise these compounds, and methods of using them to treat cancer in mammals.

Abstract: The invention relates to novel ?1-pyrrolines of the formula (I) in which R1, R2, R3, R4, A1, A2, R5, R6, R7, R8, R9 and Q are as defined in the disclosure, to a process for preparing these compounds and to their use for controlling pests.

Abstract: A method of nitrating a compound selected from the group consisting of is provided.

Abstract: The present disclosure relates to compounds used as direct dyes, and dyeing compositions comprising such compounds. The disclosed compounds have the formula A-L-B, wherein A and B are chosen from arylazoimidazolium coloring functional groups, and L is a linker comprising at least one cationic group C. The disclosure also relates methods of using such compositions for coloring keratin fibers, such as the hair.

Abstract: The present invention relates to novel compounds (I), their prodrugs, and the pharmaceutically acceptable salts as well as pharmaceutical compositions containing such compounds useful in treating certain metabolic diseases and diseases modulated by the inhibition of the enzyme malonyl-coenzyme A decarboxylase (malonyl-CoA decarboxylase, MCD). In particular, the invention relates to compounds and compositions and the methods for the prophylaxis, management and treatment of cardiovascular diseases, diabetes, acidosis, cancers, and obesity through the inhibition of malonyl-coenzyme A decarboxylase.

Abstract: The invention relates to compounds of the general formula wherein R1, R2, R3, R4, R5, R6, R7, X, Y and a have the significances given in the patent, and optionally the enantiomers thereof. The active ingredients have advantageous pesticidal properties. They are especially suitable for controlling parasites on warm-blooded animals.

Abstract: Compounds of the formula (I) in which R1, R2, R3 and R4 are as defined in Claim 1, are ligands of the nicotinic acetylcholine receptor and/or serotonergic ligands and are suitable for the prophylaxis or treatment of psychoses, schizophrenia, depression, anxiety states, dementia, in particular Alzheimer's disease and Lewy bodies dementia, neurodegenerative disorders, Parkinson's disease, amyotrophic lateral sclerosis, Huntington's disease, Tourette's syndrome, learning and memory restrictions, bulimia, anorexia nervosa or other eating disorders, compulsive behaviour, pre-menstrual syndrome, age-induced memory impairment, amelioration of withdrawal symptoms in nicotine dependence. Strokes or brain damage by toxic compounds, and for the treatment of disorders which are characterised by an excess of circulating serotonin or by serotonergic hyperactivity.

Abstract: The present invention relates to benzopyran derivatives substituted with secondary amines including imidazole, their preparation, and pharmaceutical compositions containing them. The present invention is pharmacologically useful for the treatment of cancer, rheumatoid arthritis, and diabetic retinopathies through anti-angiogenic properties, and also pharmacologically useful in the protection of heart and neuronal cells against ischemia-reperfusion injury or preserving organs.

Abstract: Compounds effective as IP receptor modulators, particularly IP receptor antagonists, that are of the formula I: wherein A, R1, R2, R3 and R4 are as defined in the specification; and individual isomers, racemic or non-racemic mixtures of isomers, and pharmaceutically acceptable salts or solvates thereof. Also disclosed are pharmaceutical compositions containing such compounds and methods for their use as therapeutic agents.

Abstract: Compounds having the general structure and compositions containing them, for the treatment of acute, inflammatory and neuropathic pain, dental pain, general headache, migraine, cluster headache, mixed-vascular and non-vascular syndromes, tension headache, general inflammation, arthritis, rheumatic diseases, osteoarthritis, inflammatory bowel disorders, inflammatory eye disorders, inflammatory or unstable bladder disorders, psoriasis, skin complaints with inflammatory components, chronic inflammatory conditions, inflammatory pain and associated hyperalgesia and allodynia, neuropathic pain and associated hyperalgesia and allodynia, diabetic neuropathy pain, causalgia, sympathetically maintained pain, deafferentation syndromes, asthma, epithelial tissue damage or dysfunction, herpes simplex, disturbances of visceral motility at respiratory, genitourinary, gastrointestinal or vascular regions, wounds, burns, allergic skin reactions, pruritus, vitiligo, general gastrointestinal disorders, gastric ulceration, d

Abstract: Imidazole compounds, compositions, and methods of using them in leukocyte recruitment inhibition, in modulating H4 receptor expression, and in treating conditions such as inflammation, H4 receptor-mediated conditions, and related conditions.

Abstract: The invention provides substituted pyrazolidinone compounds, and methods of treatment and pharmaceutical compositions that utilize or comprise one or more such compounds. Compounds of the invention are useful for a variety of therapies, including treating or preventing various cancers, inflammation, septic shock, preterm labor, infertility, pain, and ischemia, and other diseases and disorders associated with MEK-1 and/or ERK-2 activation.

Abstract: The invention provides novel inhibitors of IAP that are useful as therapeutic agents for treating malignancies where the compounds have the general formula I: wherein X, Y, A, R1, R2, R3, R4, R4?, R5, R5?, R6 and R6? are as described herein.

Abstract: A method of synthesizing aromatic ketone compositions of formula I comprising the step of introducing a double bond into the 5 membered ring of the 4,5-dihydro-1,3-azoles moiety of formula II is disclosed. A method of synthesizing aromatic ketone compositions of formula I comprising the step of ring synthesis of the tetrahydro-1,3-azoles of formula XI is also disclosed.

Abstract: The present invention relates to new compounds of formula 1, the preparation thereof, intermediate products for preparing them and the use of the compounds of formula 1 as catalysts in various metathesis reactions The new metathesis catalysts, which are obtained from readily accessible preliminary products, have a high activity and can be used for all kinds of metathesis reactions.

Abstract: Benzoyl derivatives of the formula I where the variables have the following meanings: R1, R2 are hydrogen, nitro, halogen, cyano, alkyl, haloalkyl, alkoxy, haloalkoxy, alkylthio, haloalkylthio, alkylsulfinyl, haloalkylsulfinyl, alkylsulfonyl or C1–C6-haloalkylsulfonyl; R3 is hydrogen, halogen or alkyl; R4, R5 are hydrogen, halogen, cyano, nitro, alkyl, alkoxy, alkylthio, dialkylamino, phenyl or carbonyl, it being possible for the 6 last-mentioned radicals to be substituted; X is O, S, NR9, CO or CR10R11; Y is O, S, NR12, CO or CR13R14; R15 is pyrazole which is unsubstituted or substituted, linked in the 4-position and has attached to it in the 5-position a hydroxyl or sulfonyloxy radical; and the agriculturally useful salts thereof; processes and intermediates for the preparation of the 3-heterocyclyl-substituted benzoyl derivatives, compositions comprising them; and the use of these derivatives or compositions comprising them for controlling undesirable plants.

Abstract: The invention relates to novel antifungal compounds and its pharmaceutically acceptable salts, having as part of its structure, imidazolyl or benzimidazolyl derivatives. The imidazolyl derivative may be substituted at 2 position from among the group consisting of aroyl, p-chloroaroyl, phenyl hydroxy methine or p-chloro phenyl hydroxy methine or with n-butyl at 2 position and chlorine at 4 and 5 position. In the alternative, when it is a benzimadazolyl derivative, with hydrogen at 6 position, the substituent at 2 position may be selected from among methyl, ethyl, isopropyl, 2-oxopropl-1-yl, n-propyl, methoxy methyl, propen-1-yl, phenyl, p-chlorophenyl, p-toluyl, benzyl, 4-pyridyl, p-methoxy phenyl, 3-pyridyl, o-methoxy phenyl, styryl, 2-cyano methyl, p-hydroxy phenyl, p-amino phenyl, p-toluyl sulfonyl methyl or p-(t-butyl) phenyl group and if hydrogen is at 2 position, the substituent at the 6 position is selected from among nitro, trifluoromethyl or methoxy group.

Abstract: The present invention is concerned with compounds of formula the N-oxides, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein R1 is hydrogen, hydroxy, C1-6alkyl or aryl; R2 is hydrogen; optionally substituted C1-12alkyl; C3-7cycloalkyl; C2-8alkenyl, optionally substituted pyrrolidinyl or aryl; R3 is hydrogen, optionally substituted C1-6alkyl or aryl; Het is an optionally substituted unsaturated heterocycle selected from imidazolyl, triazolyl, tetrazolyl and pyridinyl; is an optionally substituted unsaturated mono- or bicyclic heterocycle; and aryl is optionally substituted phenyl. The present invention also relates to processes for their preparation and compositions comprising said new compounds, as well as their use as a medicine.

Abstract: A process for preparing an optionally substituted 4-benzimidazol-2-ylmethylamino)benzamidine, the process comprising: (a) condensing an optionally suitably substituted diaminobenzene with 2-[4-(1,2,4-oxadiazol-5-on-3-yl)phenylamino]acetic acid; (b) hydrogenating the product obtained from step (a); and (c) optionally carboxylating the amidino group of the product obtained from step (b).

Abstract: The invention relates to compounds, pharmaceutical compositions and methods of using compounds of the general formula or its pharmaceutically acceptable salt or ester, wherein the substituents are defined in the application.

Abstract: A process for preparing telmisartan by reacting 2-n-propyl-4-methyl-6-(1?-methylbenzimidazol-2?-yl)benzimidazole with a compound of formula (IV) wherein Z is a leaving group, to obtain the compound 2-cyano-4?-[2?-n-propyl-4?-methyl-6?-(1??-methylbenzimidazol-2??-yl)benzimidazol-1?-ylmethyl]biphenyl, and subsequently hydrolyzing the nitrile function to obtain the acid function.

Abstract: Melanocortin receptor-specific pyrrolidine compounds having the structure: and stereoisomer and pharmaceutically acceptable salts thereof, where R1, R2, and R3 are as described in the specification, preferably where R3 is a D-amino acid with at least one substituted or unsubstituted phenyl or naphthyl aromatic ring, and where R3 optionally further includes an amine capping group or from one to three additional amino acid residues, optionally with an amine capping group, which compounds are agonists, antagonists or mixed agonists and antagonists at one or more melanocortin receptors, and having utility in the treatment of melanocortin receptor-related disorders and conditions. Methods of synthesis of compounds of structure (I), pharmaceutical compositions containing a compound of structure (I) and methods relating to the use thereof are also disclosed.

Abstract: Halogenated carboxylic ester derivatives of phenylethyl imidazole, and their method of preparation are disclosed. Radio-halogenated forms of these compounds are ideally suited for positron-imaging of the adrenal glands, as it is known that these compounds demonstrate a selective and high rate of accumulation in the adrenals. The method of preparing these derivatives proceeds by the conversion of a stable, non-radioactive intermediate having trialkylstannyl leaving groups. These intermediates are efficiently converted to the corresponding halogenated forms by substitution of the trialkylstannyl group with the halogen or radiohalogen.

Abstract: In its many embodiments, the present invention provides a novel class of imidazo[1,2-a] pyrazine compounds as inhibitors of cyclin dependent kinases, methods of preparing such compounds, pharmaceutical compositions containing one or more such compounds, methods of preparing pharmaceutical formulations comprising one or more such compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more diseases associated with the CDKs using such compounds or pharmaceutical compositions.

Abstract: Processes for using a compound of formula III: to make compounds of formulae I and II: and processes for making the compound of formula III, where R1-5 and J are as defined herein.

Abstract: Compounds of formula (I) are antibacterial or antiprotozoal agents for treatment of infections in humans and non-human mammals, wherein: Z represents a radical of formula —N(OH)CH(?O) or formula C(?O)NH(OH); R1 represents hydrogen, methyl or trifluromethyl, or except when Z is a radical of formula —N(OH)(?O), a hydroxy, halo or amino group; R2 represents a group R10—(X)n-(ALK)m— wherein R10, ALK, X, m and n are as defined in the specification; R3 represents hydrogen, (C1–C6) alkyl or phenyl(C1–C6)alkyl-; and R5 and R6 are as defined in the specification.

Abstract: This invention relates to novel compounds which are thyroid receptor ligands, preferably antagonists, and to methods for using such compounds in the treatment of cardiac and metabolic disorders, such as cardiac arrhythmias, thyrotoxicosis, subcllinical hyperthyrodism and liver diseases.

Abstract: This invention relates to compounds of the following formula: in which R1, R2, A1, A2, X, Y, m, n, p, x and y are as defined herein, pharmaceutical compositions comprising the compounds and use of the compounds in treating enterovirus infection.

Abstract: Imidazolium salts are the immediate precursors to N-heterocyclic carbenes (NHC) yet a simple, general synthetic route to a wide variety of imidazolium salts is not yet available. Such a straightforward route is described for two specific members of this family of ligand precursor: 1,3-Bis(2,4,6-trimethylphenyl)imidazolium chloride (IMes.HCl) and 1,3-Bis(2,6-diispropylphenyl)imidazolium chloride (IPr.HCl). The procedure appears general and similar protocols can be used to isolate various imidazolium salts.

Abstract: A cocatalyst or cocatalyst component, including a compound corresponding to the formula: (A*+a)b(Z*J*j)?cd, wherein: A* is a cation of from 1 to 80 atoms, not counting hydrogen atoms, Z* is an anion group of from 1 to 50 atoms, not counting hydrogen atoms, containing two or more Lewis base sites; J* is a Lewis acid of from 1 to 80, not counting hydrogen atoms, coordinated to at least one Lewis base site, and optionally two or more such J* groups may be joined together in a moiety having multiple Lewis acidic functionality, j is from 2 to 12 and a, b, c, and d are integers from 1 to 3, with the proviso that a×b is equal to c×d, and provided further that one or more of A*, Z* or J* comprises a hydroxyl group or a polar group containing quiescent reactive functionality.