Abstract: The present invention relates to a process for preparing a porphyrin of formula (I), optionally in the form of a salt with an alkali metal and/or in the form of a metal complex: in which: R and R? are as defined in claim 1, comprising: a step of condensation, in an acidic medium, between a dipyrromethane of formula (II): in which R?b is as defined above for (I), and a dipyrromethane of formula (III): in which R? is as defined in claim 1, and also the compounds of formula (III).

Abstract: This invention describes an ICE inhibitor prodrug (I) having good bioavailability. Compound I is useful for treating IL-1 mediated diseases such as rheumatoid arthritis, inflammatory bowel disease, Crohn's disease, ulcerative colitis, inflammatory peritonitis, septic shock, pancreatitis, traumatic brain injury, organ transplant rejection, osteoarthritis, asthma, psoriasis, Alzheimer's disease, myocardial infarction, congestive heart failure, Huntington's disease, atherosclerosis, atopic dermatitis, leukemias and related disorders, myelodysplastic syndrome, uveitis or multiple myeloma.

Abstract: The present invention relates to a process for the preparation of zofenopril and its pharmaceutically acceptable salts and a pharmaceutical composition thereof. The present invention also provides structurally novel compounds, which are useful intermediates in the synthesis of zofenopril.

Abstract: A metal coordination complex of a biologically active moiety and a metal is disclosed. The complex confers to the biologically active moiety an improved performance which can include potency, stability, absorbability, targeted delivery, and combinations thereof.

Abstract: The invention provides the compounds of formula (I) or pharmaceutically acceptable salts thereof. The invention also provides pharmaceutical compositions comprising one or more compounds of formula I or intermediates thereof and one more of pharmaceutically acceptable carriers, vehicles or diluents. The invention further provides methods of preparation and methods of use of prodrugs including NO-releasing prodrugs, double prodrugs and mutual prodrugs comprising the compounds of formula I.

Abstract: Compounds are provided which can be useful in reducing the activity of an angiotensin-converting enzyme and thus be used to treat or prevent a renin-angiotensin aldosterone system-related disorder. These compounds include lipoic acid derivatives such as prolyl lipoic acid and pipecolinyl lipoic acid, and other compounds, and these compounds are useful in treating hypertension, stroke, or other renin-angiotensin aldosterone system-related disorders in human or animal patients. Pharmaceutical compositions prepared using these compounds and methods of treatment using these compounds are also provided.

Abstract: Provided herein are compounds of the formula (I): as well as pharmaceutically acceptable salts thereof, wherein the substituents are as those disclosed in the specification. These compounds, and the pharmaceutical compositions containing them, are useful for the treatment of metabolic diseases and disorders such as, for example, type II diabetes mellitus.

Abstract: In the present invention, a hydroxyl group substitution product is manufactured by reaction of an alcohol with sulfuryl fluoride (SO2F2) in the presence of an organic base and a nucleophile (X?). The present invention is thus effective as an industrial manufacturing method that uses a relatively cheap reagent suitable for large-scale applications and can be accomplished in a simple process with easy purification operation and less waste generation and is suitably applicable for manufacturing of optically active hydroxyl group substitution products, notably optically active ?-hydroxyl group substitution ester and optically active 4-hydroxyl group substitution proline. The manufacturing method of the present invention solves all of the prior art problems and can be applied for industrial uses.

Abstract: A process for the preparation of ?-alkoxycarbonylamino-?-aminoacids and ?,? orthogonally diprotected diaminoacids from ?,?-diaminoacids using 1-alkoxycarbonylbenzotriazoles as protecting agents is disclosed. In an alternative embodiment, carbamoylating agents in the presence of benzotriazoles are used instead of 1-alkoxycarbonylbenzotriazoles. This reaction is preferably applied to the preparation of ?-alkoxycarbonyllysines from lysine. A process for the preparation of t-butoxycarbonylbenzotriazoles and novel complexes of ?-alkoxycarbonylamino-?-aminoacids with benzotriazoles are also disclosed.

Abstract: Fluorosulfuric acid esters can be produced by reacting alcohols with sulfuryl fluoride (SO2F2) in the presence of a base and water. As a substrate thereof, optically active secondary alcohols are preferable, and optically active ?-hydroxyesters and optically active 4-hydroxyprolines are particularly preferable. By performing the reaction in a two-phase system in the presence of a reaction solvent immiscible with water, a desired reaction proceeds particularly well. The present invention is a production method solving all the problems involved in conventional techniques while being industrially practicable.

Abstract: This invention relates to neurotrophic compounds having an affinity for FKBP-type immunophilins, their preparation and use as inhibitors of the enzyme activity associated with immunophilin proteins, and particularly inhibitors of peptidyl-prolyl isomerase or rotamase enzyme activity.

Abstract: Disclosed is a process of forming a pyrrole compound. The process comprises contacting an ?-carbonyl oxime compound 1 and an ?,?-unsaturated aldehyde 2 R1 and R2 in compound 1 are independently selected from the group consisting of H, a silyl-group, an aliphatic group, an alicyclic group, an aromatic group, an arylaliphatic group, and an arylalicyclic group. The aliphatic, alicyclic, aromatic, arylaliphatic, and arylalicyclic groups comprise 0 to about 3 heteroatoms selected from the group N, O, S, Se and Si. R3 in aldehyde 2 is selected from the group consisting of H, a silyl-group, an aliphatic group, an alicyclic group, an aromatic group, an arylaliphatic group, and an arylalicyclic group. The aliphatic, alicyclic, aromatic, arylaliphatic, and arylalicyclic groups comprise 0 to about 3 heteroatoms selected from the group N, O, S, Se and Si. The ?-carbonyl oxime compound 1 an the ?,?-unsaturated aldehyde 2 are contacted in a suitable solvent in the presence of a secondary amine.

Abstract: Provided herein are compounds of the formula (I): as well as pharmaceutically acceptable salts thereof, wherein the substituents are as those disclosed in the specification. These compounds, and the pharmaceutical compositions containing them, are useful for the treatment of metabolic diseases and disorders such as, for example, type II diabetes mellitus.

Abstract: The present invention relates to two novel crystalline forms of zofenopril calcium, to processes for their preparation and their use in pharmaceutical compositions.

Abstract: Overexpression of angiotensin-converting enzyme (ACE) has been associated with a number of pathophysiologies, including those associated with cancer and the cardiovascular system. Thus, targeted imaging of ACE is of crucial importance for monitoring tissue ACE activity as well as treatment efficacy. To this end, lisinopril-coated gold nanoparticles were prepared to provide a new type of probe for targeted molecular imaging of ACE by tuned K-edge computed tomography (CT) imaging.

Abstract: What is described are the compounds and the synthesis of [F-18]-labelled L-glutamic acid, [F-18]-labelled L-glutamate, their derivatives of the formula (I) and their use.

Abstract: A method for making a surfactant-based monolithic column is provided. The method comprises providing a mixture comprising at least one surfactant monomer, at least one crosslinker, at least one initiator, and at least one porogen and polymerizing the mixture to form the surfactant-based monolithic column. The present disclosure also provides a surfactant-based monolithic column, a method for separating molecules, and a process for preparing a surfactant monomer.

Abstract: Processes using Allium tissue homogenates and extracts in a simple and cost-effective manner to maximize the yields and recovery of thiosulfinates from Allium tissues and related organisms possessing alliinase, LF synthase and/or S-alk(en)yl-L-cysteine sulfoxides are disclosed.

Abstract: A process for separating the diastereomers of RSS— and SSS—N-?[1-carboxy-3-phenylpropyl]lysylproline is described. Previous chromatographic processes for separating the diastereomers of this peptide active substance, such as for example adsorption chromatography, exhibited disadvantages with regard to the solvents used and throughput. These disadvantages do not occur if basic ion exchangers are used in the chromatographic separation of the diastereomers. In particular, purely aqueous solutions may be used as the eluent.

Abstract: The present invention provides a photoresist composition comprising a resin, an acid generator and a compound represented by the formula (I): wherein R1 represents a C2-C12 alkyl group which can have one or more hydroxyl groups, etc., R2 and R3 each independently represent a hydrogen atom, etc., R4, R5 and R6 each independently represent a hydrogen atom, etc., A1 represents a single bond or a C1-C2 alkylene group in which one or more —CH2— can be replaced by —O—.

Abstract: The present invention provides a compound represented by the formula (C1): wherein Rc2 represents a C6-C10 aromatic hydrocarbon group having at least one nitro group and Rc1 represents a group represented by the formula (1): wherein Rc4 represents a hydrogen atom etc., Rc5 represents a C1-C30 divalent hydrocarbon group, and Rc3 represents a group represented by the formula (3-1), (3-2) or (3-3): wherein Rc6, Rc7, Rc8, Rc9, Rc10, Rc11, Rc12, Rc13 and Rc14 each independently represent a C1-C30 hydrocarbon group, and a photoresist composition comprising a resin, an acid generator and the compound represented by the formula (C1).

Abstract: The present invention relates to zofenopril calcium form A substantially free of other forms of zofenopril calcium and to zofenopril calcium having a chemical purity of more than 98.5%. The present invention also relates to methods of preparing such zofenopril calcium. It further relates to compositions comprising such zofenopril calcium.

Abstract: Gelling agents which contain a specific N-acylamino acid monoamide monoalkyl ester have a melting temperature of about 100° C., are capable of solidifying a wide variety of oily base materials including silicones, and do not cause “sweating” while retaining a practical level of gel strength. When applied to skin, the resulting gels have a good feeling, good spreadability, and good fittability to skin.

Abstract: What is described are the compounds and the synthesis of [F-18]-labelled L-glutamic acid, [F-18]-labelled L-glutamate, their derivatives of the formula (I) and their use.

Abstract: Provided are methods for the preparation of certain substituted pyrrolidine compounds, forms of (2S,4R)-1-(2-aminoacetyl)-4-benzamidopyrrolidine-2-carboxylic acid hydrochloride, and methods for preparing and using these forms.

Abstract: A family of N-substituted 3,4-alkylenedioxypyrrole includes monomers for of formula (I) electropolymerization to conjugated polymers and key intermediates for the preparation of the monomers. The preparation of the //-substituted 3,4-alkylenedioxypyrroles is carried out via a synthetic intermediate, an ester substituted dihydroxypyrrole. The synthetic method to prepare the //-substituted 3,4-alkylenedioxypyrrole intermediates and ultimately the N-substituted 3,4-alkylenedioxypyrrole monomers begins with a reaction to form the ester substituted dihydroxypyrrole.

Abstract: A novel process of preparing allyl-containing asymmetric disulfides, and particularly therapeutically active allyl-containing asymmetric disulfides such as allylmercaptocaptopril (CPSSA) is disclosed.

Abstract: This disclosure describes the molecular cloning of a pactamycin biosynthetic gene cluster from Streptomyces pactum ATCC 27456, characterization of individual genes in the gene cluster and the proteins encoded thereby as well as uses thereof. The pactamycin gene cluster is located within an 86.35 kilobases genetic locus and includes 53 open reading frames, 26 of which are considered to be the core cluster directly involved in the biosynthesis of pactamycin.

Abstract: Among other things, the present invention provides novel isoprenyl compounds capable of effectively modulating inflammatory responses and pharmaceutical, cosmetic, cosmeceutical and topical compositions comprising these isoprenyl compounds. Anti-inflammatory compounds of the present invention are useful in treating or preventing diseases or conditions associated with inflammation. Proinflammatory compounds of the present invention are useful in treating or preventing diseases or conditions associated with suppression of inflammatory responses. Thus, the present invention also provides methods useful in the treatment or prevention of diseases or conditions associated with inflammation as well as methods useful in the treatment or prevention of diseases or conditions associated with suppression of inflammatory responses.

Abstract: Useful industrial methods for producing optically active fluoropyrrolidine derivatives as useful fluorinated intermediates are disclosed.

Abstract: The invention relates to novel 2-alkoxy-6-alkylphenyl-substituted spirocyclic tetramic acid derivatives of the formula (I) in which A, B, D, G, X, Y and Z are as defined above, to a plurality of processes and intermediates for their preparation and to their use as pesticides and/or herbicides, and also to selective herbicidal compositions comprising, firstly, the 2-alkoxy-6-alkylphenyl-substituted spirocyclic tetramic acid derivatives of the formula (I) and, secondly, at least one crop plant tolerance promoter compound.

Abstract: The present application discloses conjugates comprising an aminic moiety covalently linked to a hydrophobic moiety, through an amidic bond, which are selective inhibitors of COX-2 enzyme and can be beneficially used in the treatment of various inflammatory disease or disorder and cancer.

Abstract: This invention relates to neurotrophic compounds having an affinity for FKBP-type immunophilins, their preparation and use as inhibitors of the enzyme activity associated with immunophilin proteins, and particularly inhibitors of peptidyl-prolyl isomerase or rotamase enzyme activity.

Abstract: The invention provides novel compounds of general formula I wherein R1, R2 and R3 are independently hydrogen, OR4, C1-C6 alkyl or C2-C6 alkenyl, R4 is hydrogen, C1-C6 alkyl or C2-C6 alkenyl, —N-(AA) represents the residue of an amino acid or of a peptide which is bonded over the N-terminus of the amino acid or the peptide and the peptide is composed of 2 to 6, that means 2, 3, 4, 5 or 6, amino acids, wherein the C-terminus of the amino acid or the peptide is optionally esterified with a C1-C16 hydrocarbon moiety and n is an integer of 1 to 5. The compounds are in particular useful for cosmetic applications.

Abstract: Compounds of formula (I): or pharmaceutically acceptable salts and esters thereof, are useful for the treatment of obesity, type II diabetes and the metabolic syndrome.

Abstract: Methods of inhibiting HSP70 proteins, agents causing the inhibition of HSP70 proteins, and the effects of such inhibition on cell proliferation. Anti-microbial agents comprising small molecules, or pharmaceutical salts thereof, disclosed herein and further methods of use thereof are also disclosed. The disclosed small molecules, or pharmaceutical salts thereof, are effective in inhibiting microbial chaperone activity in microbes, such as homologs of HSP70. The disclosed small molecules, or pharmaceutical salts thereof, are also effective for the therapeutic treatment of cancer.

Abstract: This invention relates to neurotrophic compounds having an affinity for FKBP-type immunophilins, their preparation and use as inhibitors of the enzyme activity associated with immunophilin proteins, and particularly inhibitors of peptidyl-prolyl isomerase or rotamase enzyme activity.

Abstract: Compounds of the formula provide pharmacological agents which bind to Peroxisome Proliferator-Activated Receptors (PPARs). Accordingly, the compounds of the instant invention are useful for the treatment of conditions mediated by the PPAR receptor activity in mammals. Such conditions include dyslipidemia, hyperlipidemia, hypercholesteremia, atherosclerosis, hypertriglyceridemia, heart failure, myocardial infarction, vascular diseases, cardiovascular diseases, hypertension, obesity, inflammation, arthritis, cancer, Alzheimer's disease, skin disorders, respiratory diseases, ophthalmic disorders, inflammatory bowel diseases, ulcerative colitis, Crohn's disease, and conditions in which impaired glucose tolerance, hyperglycemia and insulin resistance are implicated, such as type-1 and type-2 diabetes, and Syndrome X.

Abstract: The present invention relates to a cycloalkene derivative represented by the formula (I): wherein each symbol is as defined in the specification, a pharmaceutical agent containing the derivative, and a production method thereof. The cycloalkene derivative of the present invention has high solubility in water and is suitable for use as an injection.

Abstract: The present invention relates to zofenopril calcium form A substantially free of other forms of zofenopril calcium and to zofenopril calcium having a chemical purity of more than 98.5%. The present invention also relates to methods of preparing such zofenopril calcium. It further relates to compositions comprising such zofenopril calcium.

Abstract: A family of N-substituted 3,4-alkylenedioxypyrrole includes monomers for of formula (I) electropolymerization to conjugated polymers and key intermediates for the preparation of the monomers. The preparation of the //-substituted 3,4-alkylenedioxypyrroles is carried out via a synthetic intermediate, an ester substituted dihydroxypyrrole. The synthetic method to prepare the //-substituted 3,4-alkylenedioxypyrrole intermediates and ultimately the N-substituted 3,4-alkylenedioxypyrrole monomers begins with a reaction to form the ester substituted dihydroxypyrrole.

Abstract: The present invention relates to N-cyclopropyl-sulfonylamide derivatives of formula (I) wherein the substituents are cyclic groups, their process of preparation, their use as fungicide active agents, particularly in the form of fungicide compositions, and methods for the control of phytopathogenic fungi, notably of plants, using these compounds or compositions: (I)

Abstract: Hydride process for making acyclic diol intermediates from cyclic intermediates, useful in antibacterial quinolone synthesis.

Abstract: The present invention provides a compound of the general formula (I), wherein X is the connection between the CO-hydrazine and the NR1-oxalic acid or ester group, and uses and synthesis methods. These compounds represent amino acid derivatives, wherein the amine group is turned into an acidic group by the oxalic acid group and the carboxylic acid is turned into an amine functionality by the hydrazine group; as well as peptidomimetics comprising the compound and methods for their synthesis.

Abstract: The invention provides small molecule mimics of the Smac peptide that are dimer-like or trimer-like compounds having two or three amide-containing domains connected by a linker. These compounds are useful to promote apoptosis. The invention includes pharmaceutical compositions comprising such compounds and methods to use them to treat conditions including cancer and autoimmune disorders.

Abstract: Compounds of formula (I): (A)m·(B)n??(I) wherein A represents an angiotensin-converting enzyme inhibitor compound containing at least one salt-forming basic function, B represents a compound containing at least one salt-forming acid function and at least one NO donor group, m represents the number of acid functions of B that have been converted to a salt and n represents the number of basic functions of A that have been converted to a salt, the bond or bonds between A and B being of the ionic type. Medicinal products containing the same which are useful in treating cardiovascular pathologies.

Abstract: The present invention relates to compounds that are capable of inhibiting, modulating and/or regulating signal transduction of both receptor-type and non-receptor type tyrosine kinases. The compounds of the instant invention possess a core structure that comprises a substituted pyrrole moiety. The present invention is also related to the pharmaceutically acceptable salts, hydrates and stereoisomers of these compounds.

Abstract: This invention describes an ICE inhibitor prodrug (I) having good bioavailability. Compound I is useful for treating IL-1 mediated diseases such as rheumatoid arthritis, inflammatory bowel disease, Crohn's disease, ulcerative colitis, inflammatory peritonitis, septic shock, pancreatitis, traumatic brain injury, organ transplant rejection, osteoarthritis, asthma, psoriasis, Alzheimer's disease, myocardial infarction, congestive heart failure, Huntington's disease, atherosclerosis, atopic dermatitis, leukemias and related disorders, myelodysplastic syndrome, uveitis or multiple myeloma.

Abstract: The invention related to a novel process, novel process steps and novel intermediates useful in the synthesis of pharmaceutically active compounds, especially renin inhibitors, such as Aliskiren. Inter alia, the invention relates to a process for the manufacture of a compound of the formula III, wherein R, R1, and R? are as defined in the specification, or a salt thereof, and a compound of formula IV wherein R, R1, R2 and R? are as defined in the specification, and processes of manufacturing these.

Abstract: The invention relates to a compound having general formula I, wherein: X represents CH2, C?O, C?S or CHOH, X represents CH2, C?O, C?S or CHOH, R1 represents an amino acid which is optionally substituted by one or more halogen atoms, preferably fluorine, or by one or more CF3 groups and n=0.1 or 2, or X represents CH2, C?O, C?S, CHOH, R1 represents a peptide containing two amino acids, each amino acid being optionally substituted by one or more halogen atoms, preferably fluorine, or by one or more CF3 groups and n=0 or 1, or XR1 represent PO3H or SO3H and n=0.