Abstract: The present disclosure relates to the field of pharmaceutical synthesis, and more particularly, relates to a monocyclic ?-lactam-siderophore conjugate as well as a method for synthesizing same and its use in the treatment of bacterial infectious diseases. Provided are a monocyclic ?-lactam-siderophore conjugate represented by formula (I) as described herein, an optical isomer thereof or a pharmaceutically acceptable salt thereof, and a method for synthesizing same, and a use thereof in treating bacterial infectious diseases.

Abstract: The invention provides a non-naturally occurring microbial organism having an adipate, 6-aminocaproic acid or caprolactam pathway. The microbial organism contains at least one exogenous nucleic acid encoding an enzyme in the respective adipate, 6-aminocaproic acid or caprolactam pathway. The invention additionally provides a method for producing adipate, 6-aminocaproic acid or caprolactam. The method can include culturing an adipate, 6-aminocaproic acid or caprolactam producing microbial organism, where the microbial organism expresses at least one exogenous nucleic acid encoding an adipate, 6-aminocaproic acid or caprolactam pathway enzyme in a sufficient amount to produce the respective product, under conditions and for a sufficient period of time to produce adipate, 6-aminocaproic acid or caprolactam.

Abstract: Process for the preparation of intermediates useful in the synthesis of miglustat and their use in its manufacture.

Abstract: The present invention relates to novel carboxamide compounds and their use for the manufacture of a medicament. The carboxamide compounds are inhibitors of calpain (calcium dependant cysteine proteases). The invention therefore also relates to the use of these carboxamide compounds for treating a disorder associated with an elevated calpain activity. The carboxamide compounds are compounds of the general formula I in which R1, R2, R3a, R3b, R4, Q, Y, A and X have the meanings mentioned in the claims and the description, the tautomers thereof and the pharmaceutically suitable salts thereof. In particular, the compounds have the general formula Ia and Ib in which R1, r, R2b, R3a, R3b, R4, Y and X have the meanings mentioned in the claims, including the tautomers thereof and the pharmaceutically suitable salts thereof.

Abstract: The present invention relates to a method for preparing lactams using heterogeneous catalysis by hydrogenating at least one compound of the following formula (I), where A is a radical of the following formula (I?) or (II?): —CH(R1)—CH(R2)— (I?); or —CH(R1)—CH(R2)—CH(R3)— (II?); where R1, R2 and R3 are, independently from each other, H, OH, an alkyl radical, or a cycloalkyl radical; and R is H or a straight or branched alkyl radical having 1 to 20, preferably 1 to 10, and more preferably 1 to 4 carbon atoms. Said method is carried out at a pressure of less than 60 bars, preferably 10 to 50 bars, in the presence of a solid hydrogenation catalyst including at least two metals selected from the group of noble metals and transition metals, and an inert substance used as a support, wherein said compound of formula (I) can be used alone or as part of a mixture.

Abstract: The present invention allows formation of covalent bonds in a bioactive compound having at least one amino group so as to efficiently provide the compound modified with PEG. The present invention thus provides a functionalized polyethylene glycol having a structure that allows reaction of two aldehyde groups with one amino group to form two covalent bonds.

Abstract: Process for the preparation of animinosugar, and the intermediates thereof, having known activity as a glycosyltransferase inhibitor and used, for example, in the treatment of Gaucher's disease.

Abstract: The present invention relates to novel compounds, compositions containing same and methods for inhibiting human farnesyl pyrophosphate synthase or for the treatment or prevention of disease conditions using said compounds;

Abstract: The present invention relates to a novel method for preparing a compound of formula (2) as the intermediate, which can be effectively used for preparation of a compound of formula (1) exhibiting good inhibitory activity against dipeptidyl peptidase IV enzyme.

Abstract: The invention described herein pertains to compounds and compositions for treating Ape1 mediated diseases. In particular, the invention described herein pertains to quinone compounds and pharmaceutical compositions containing them for treating Ape1 mediated diseases.

Abstract: The present invention is directed to compounds represented by structural formula (I), or a pharmaceutically acceptable salt or a transition metal chelate, coordinate or complex thereof or a transition metal chelate, coordinate or complex of a deprotonated form of the compound. Pharmaceutical composition and method of use for these compounds are also included.

Abstract: Herein are described compounds having a structure or a pharmaceutically acceptable salt thereof, wherein Y, A, and B are as described. Methods, compositions, and medicaments related thereto are also disclosed.

Abstract: The present invention relates generally to pharmaceutical agents, and in particular, to metalloprotease inhibitor compounds. More particularly, the present invention provides a new class of dual acting MMP-2 and MMP-9 inhibiting compounds that exhibit increased potency, metabolic stability and/or reduced toxicity in relation to currently known MMP-2 and MMP-9 inhibitors for the treatment of pain and other diseases. Additionally, the present invention relates to methods for treating pain, addiction and/or withdrawal symptoms in a patient comprising administering to the patient a pain-reducing effective amount of a present compound.

Abstract: A process for the preparation of imides and also the uses thereof, especially as intermediates for the preparation of solvents, in particular of diester solvents, is described. Further described is a process for preparing cyclic imides and derivatives thereof, especially the corresponding carboxylic acids.

Abstract: The production of compounds comprising nitrile functions and of cyclic imide compounds is described. Further described, is the production of compounds comprising nitrile functions from compounds comprising carboxylic functions, optionally of natural and renewable origin, and from a mixture N of dinitriles comprising 2-methylglutaronitrile (MGN), 2-ethylsuccinonitrile (ESN) and adiponitrile (AdN).

Abstract: The invention relates to the generation of a library of compounds enriched in agonist and antagonists for members of the G-protein coupled class of receptors (GPCRs). The library contains compounds of general formula (II) wherein: y is any integer from 1 to 8; X is —CO—R1 or —SO2—R1; each R1 is independently selected from an alkyl, haloalkyl, alkenyl, alkynyl, alkylaminoalkyl, alkylaminodialkyl, or charged alkylaminotrialkyl, radical of 1 to 20 carbon atoms; or each R1 is independently selected from oxyalkyl, aminoalkyl, aminodialkyl, or charged aminotrialkyl radical; and wherein the R1 radical has a “key” carbon next to the carbonyl of the carbon amide or the sulfonyl group of the sulfonamide which is di-substituted with the same or different groups selected from: alkyl, haloalkyl, alkoxy, haloalkoxy, alkenyl, alkynyl and alkylamino radicals.

Abstract: The present invention relates to novel carboxamide compounds and their use for the manufacture of a medicament. The carboxamide compounds are inhibitors of calpain (calcium dependant cysteine proteases). The invention therefore also relates to the use of these carboxamide compounds for treating a disorder associated with an elevated calpain activity. The carboxamide compounds are compounds of the general formula I in which R1, R2, R3a, R3b, R4, Q, Y, A and X have the meanings mentioned in the claims and the description, the tautomers thereof and the pharmaceutically suitable salts thereof. In particular, the compounds have the general formula Ia and Ib in which R1, r, R2b, R3a, R3b, R4, Y and X have the meanings mentioned in the claims, including the tautomers thereof and the pharmaceutically suitable salts thereof.

Abstract: A sulfonic acid onium salt represented by the following formula (1) can be used as a superior radiosensitive acid generator for resist compositions. It is possible to form a good pattern by using a resist composition containing this sulfonic acid onium salt. In formula (1), R1 represents a monovalent organic group, and Q+ represents a sulfonium cation or iodonium cation.

Abstract: A process for transforming a group >C?O (I) in a compound into a group >C?S (II) or into a tautomeric form of group (II) in a reaction giving a thionated reaction product, by use of crystalline P2S5.2 C5H5N as a thionating agent. A thionating agent which is crystalline P2S5.2 C5H5N.

Abstract: Compounds of the formula I: or pharmaceutically acceptable salts thereof, wherein m, n, R1, R2, R3, R4, R5 and Ra are as defined herein. Also disclosed are methods of making the compounds and using the compounds for treatment of diseases associated with the P2X7 purinergic receptor.

Abstract: Novel compounds are provided which are GPR119 G protein-coupled receptor modulators. GPR119 G protein-coupled receptor modulators are useful in treating, preventing, or slowing the progression of diseases requiring GPR119 G protein-coupled receptor modulator therapy. These novel compounds have the structure Formula I or Formula IA.

Abstract: The present invention provides cysteine and cystine prodrugs for the treatment of schizophrenia and drug addiction. The invention further encompasses pharmaceutical compositions containing prodrugs and methods of using the prodrugs and compositions for treatment of schizophrenia and drug addiction.

Abstract: A process is provided for the synthesis of an amide. A primary or secondary amine and a primary alcohol, with the amine and the alcohol being either moieties of different reactants or moieties of the same molecule, are contacted in the presence of a Ruthenium (II) catalyst. The Ruthenium (II) catalyst is free of a phosphine ligand. The process is also carried out in the absence of a phosphine. Providing the Ruthenium (II) catalyst includes providing an N-heterocyclic carbene.

Abstract: The present application relates to novel lactam-substituted dicarboxylic acid derivatives, processes for their preparation, their use for the treatment and/or prophylaxis of diseases, and their use for producing medicaments for the treatment and/or prophylaxis of diseases, especially for the treatment and/or prevention of cardiovascular disorders.

Abstract: The present invention is directed to compounds represented by structural formula (I), or a pharmaceutically acceptable salt or a transition metal chelate, coordinate or complex thereof or a transition metal chelate, coordinate or complex of a deprotonated form of the compound. Pharmaceutical composition and method of use for these compounds are also included.

Abstract: This invention relates to an improved and scalable process for the preparation of substantially pure palonosetron and its acid addition salts, in particular hydrochloride (I) which comprises of, (a) converting intermediate (IIa) as such or as its freebase (II) to a crude mixture of diastereomeric palonosetrons (VIII) or (VIIIa) contaminated with varying amounts of unconverted intermediate (II) or (IIa) via hydrogenation under pressure with an appropriately chosen hydrogenation catalyst in an suitable organic solvent. (b) making the resulting crude mixture of diastereomeric palonosetrons (VIII) or (VIIIa) contaminated with varying amounts of unconverted intermediate (II) or (IIa) substantially free from (II) or (IIa) via halogenation reaction.

Abstract: The present invention provides, inter alia, a compound of formula I: wherein the substituent designations are indicated in the Specification. The present invention also provides pharmaceutical compositions comprising a compound of formula I, and methods of treatment or prevention of diabetes or hyperglycemia in a patient, and of normalizing blood glucose levels in a subject, by administering an effective amount of a compound of formula I.

Abstract: The invention described herein provides for novel nitric oxide-releasing polymers that comprise at least two adjacent units derived from acrylonitrile monomer units and containing at least one carbon-bound diazeniumdiolate. The diazeniumdiolated acrylonitrile-derived polymers can be used in medical devices therapeutically. Accordingly, the invention also provides a method of treating a biological disorder and a method of promoting angiogenesis that includes administering a medical device comprising a nitric oxide-releasing polymer comprising at least two adjacent units of acrylonitrile before exposure to nitric oxide and at least one nitric oxide releasing N2O2? group, wherein the N2O2? group is attached directly to the polyacrylonitrile backbone, to a specific location on or within the mammal in an amount effective to treat the biological disorder or promote angiogenesis.

Abstract: Disclosed is a parasitic plant control agent which can control a parasitic plant effectively. Also disclosed is a parasitic plant control method. A parasitic plant can be controlled by inhibiting the metabolism of gentianose in the parasitic plant to inhibit the germination of the parasitic plant.

Abstract: It is desirable to provide a method for easily removing catalyst-derived impurities from a product of a reaction by the catalysis of a compound having a dicarboximide skeleton and thereby efficiently yielding a target compound with high purity. Disclosed is a method for producing an organic compound through a reaction of a substrate in the presence of a catalyst, the catalyst including a compound having a dicarboximide skeleton represented by following Formula (i): wherein R represents hydrogen atom or a hydroxyl-protecting group. The method includes the step of treating a reaction product with hot water so as to decompose and remove an impurity derived from the catalyst. The temperature of the hot water is preferably 100° C. or higher.

Abstract: The present invention describes a novel elastomeric biodegradable photoluminescent polymer (BPLP). The BPLPs of the present invention possess great processability and tunable fluorescence emission characteristics and are cell-compatible and biodegradable. The BPLPs of the present invention can serve as both implant materials and bioimaging probes.

Abstract: A series of substituted aryl sulfone derivatives represented by Formula I, or pharmaceutically acceptable salts thereof. Pharmaceutical compositions comprise an effective amount of the instant compounds, either alone, or in combination with one or more other therapeutically active compounds, and a pharmaceutically acceptable carrier. Methods of treating conditions associated with, or caused by, calcium channel activity, including, for example, acute pain, chronic pain, visceral pain, inflammatory pain, neuropathic pain, urinary incontinence, itchiness, allergic dermatitis, epilepsy, diabetic neuropathy, irritable bowel syndrome, depression, anxiety, multiple sclerosis, sleep disorder, bipolar disorder and stroke, comprise administering an effective amount of the present compounds, either alone, or in combination with one or more other therapeutically active compounds.

Abstract: This invention provides caspase inhibitors of formula I: wherein Z is oxygen or sulfur; R1 is hydrogen, —CHN2, R, CH2OR, CH2SR, or —CH2Y; ?between R3 and R4 represents a single or double bond; Y is an electronegative leaving group; R2 is CO2H, CH2CO2H, or esters, amides or isosteres thereof; R3 is a group capable of fitting into the S2 subsite of a caspase enzyme; R4 is a hydrogen or C1-6 alkyl or R3 and R4 taken together form a ring; Ring A and Ring B are each heterocyclic rings, and R and R5 are as described in the specification. The compounds are effective inhibitors of apoptosis and IL-1? secretion.

Abstract: Described are various compounds and methods for the treatment of disorders arising from aberrant protein folding, including in particular lysosomal storage diseases. In particular, polyhydroxylated alkaloids and imino sugars which are pharmacoperones of an enzyme and which do not bind to a catalytic site of said enzyme are described.

Abstract: A process for preparing an N-alkyllactam with improved color quality, wherein from 0.01 to 10% by weight of a C1-10-alcohol or a compound which releases from 0.01 to 10% by weight of a C1-10-alcohol is added to the N-alkyllactam. A mixture comprising at least 99.0% by weight of an N-alkyllactam and in the range from 100 to 5000 ppm by weight of a C1-10-alcohol or of an acetal, aminal or of an orthoester which releases in the range from 100 to 5000 ppm by weight of a C1-10-alcohol.

Abstract: The invention relates to compounds of formula I in which A, R1, R2, R3, R4, R5, R6, R7 and n have the meanings stated in the claims. The compounds are particularly suitable as antiarrhythmic active ingredients, in particular for the treatment and prophylaxis of atrial arrhythmias, for example atrial fibrillation (AF) or atrial flutter.

Abstract: The present invention relates to new compounds, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals.

Abstract: The present application relates to novel lactam-substituted dicarboxylic acid derivatives, processes for their preparation, their use for the treatment and/or prophylaxis of diseases, and their use for producing medicaments for the treatment and/or prophylaxis of diseases, especially for the treatment and/or prevention of cardiovascular disorders.

Abstract: 1,5-Dideoxy-1,5-imino-D-glucitol compounds as shown in the specification. Also disclosed is a method of treating a hexosaminidase-associated disease.

Abstract: Disclosed herein is a compound having a structure or a pharmaceutically acceptable salt, prodrug, or bioisostere thereof. Therapeutic methods, compositions, and medicaments related thereto are also disclosed.

Abstract: A process for preparing N-alkenyl compounds by reacting the corresponding NH compounds with alkynes in the liquid phase in the presence of a catalyst, wherein the reaction is carried out in the presence of at least one stabilizer, and the use of stabilizers for increasing the selectivity in a process for preparing N-alkenyl compounds by reacting the corresponding NH compounds with alkynes in the liquid phase in the presence of a catalyst.

Abstract: The invention relates to the use of 3-(2?,2?-dimethylpropanoylamino)-tetrahydropyridin-2-one for preparing a medicament intended to prevent or treat inflammatory disorders.

Abstract: The invention provides compounds, pharmaceutical compositions and uses of compounds and salts thereof of general formula (I), for the preparation of a medicament for treatment of an inflammatory disorder, but excluding (S)-3-(r-methylcyclohexyl-carbonylamino)-caprolactam: wherein z is 1, 2, 3 or 4; A is —CO— or —SO2-; Q is linear or branched alkyl, alkenyl, alkynyl, alkoxy, oxyalkyl, aminoalkyl, alkylamino, alkylaminoalkyl, haloalkyl, aryl or substituted aryl; T1 and T2 together constitute a cycloalkyl, cycloalkenyl or polycycloalkyl radical composed of n additional carbon atoms, where n is between 2 and 7; and each hydrogen atom bonded to the carbon atoms in the ring generated by T1 and T2 may be independently be substituted by a group R1, where R1 is independently selected from an alkyl, haloalkyl, alkoxy, haloalkoxy, alkenyl, alkynyl or alkylamino radical of 1 to 20 carbon atoms; or each R1 is independently selected from fluoro, chloro, bromo, iodo, hydroxy, oxyalkyl, amino, aminoalkyl or aminodialkyl radi

Abstract: Disclosed are 2-amino-7,8-dihydro-6H-pyrido[4,3-d]pyrimidin-5-one compounds, their stereoisomers, tautomers, pharmaceutically acceptable salts, and prodrugs thereof; compositions that include a pharmaceutically acceptable carrier and one or more of the 2-amino-7,8-dihydro-6H-pyrido[4,3-d]pyrimidin-5-one compounds, either alone or in combination with at least one additional therapeutic agent. Disclosed also are methods of using the 2-amino-7,8-dihydro-6H-pyrido[4,3-d]pyrimidin-5-one compounds, either alone or in combination with at least one additional therapeutic agent, in the prophylaxis or treatment of cellular proliferative, viral, autoimmune, cardiovascular, and central nervous system diseases.

Abstract: Compounds produced by combining imino sugars and creatine are herein disclosed. The compounds being in the form of a creatine imino sugar amides and produced by the disclosed methods; protecting the guanidine group of creatine and then activating the protected creatine with DCC and reacting it with an imino sugar, followed by removal of the guanidine protecting groups. The resulting creatine imino sugar amides have enhanced stability in solution as compared to related esters. In addition, specific benefits are conferred by the imino sugar in addition to, and separate from, the creatine substituent. Methods of preparation and use of these compounds are also disclosed.

Abstract: A compound (8) represented by the formula: (8) wherein R1 represents a 6- to 14-membered aromatic hydrocarbon ring group which may have a substituent; and n represents 0 to 2, can be produced with good efficiency by reacting a compound (3) represented by the formula: (3) wherein R1 and n are as defined above; and Q represents a single bond or —CH(Y)— where Y represents a hydrogen atom or a C1-6 alkyl group] with 3-methoxy-4-(4-methyl-1H-imidazol-1-yl)benzaldehyde in the presence of a base.

Abstract: This invention provides caspase inhibitors of formula I: wherein Z is oxygen or sulfur; R1 is hydrogen, —CHN2, R, CH2OR, CH2SR, or —CH2Y; between R3 and R4 represents a single or double bond; Y is an electronegative leaving group; R2 is CO2H, CH2CO2H, or esters, amides or isosteres thereof; R3 is a group capable of fitting into the S2 subsite of a caspase enzyme; R4 is a hydrogen or C1-6 alkyl or R3 and R4 taken together form a ring; Ring A and Ring B are each heterocyclic rings, and R and R5 are as described in the specification. The compounds are effective inhibitors of apoptosis and IL-1? secretion.

Abstract: Herein are described compounds having a structure or a pharmaceutically acceptable salt thereof, wherein Y, A, and B are as described. Methods, compositions, and medicaments related thereto are also disclosed.

Abstract: The invention provides compounds, pharmaceutical compositions and uses of compounds of general formula (I) or a pharmaceutically acceptable salt thereof, for the preparation of a medicament intended to treat an inflammatory disorder; wherein z X is 1, 2 or 4; X is —CO—Yk—(R1)n or SO2—Yk—(R1)n; k is 0 or 1; Y is a cycloalkyl or polycyloalkyl group (such as an adamantyl, adamantanemethyl, bicyclooctyl, cyclohexyl, cyclopropyl group); or is a cycloalkenyl or polycycloalkenyl group; each R1 is independently selected from hydrogen or an alkyl, haloalkyl, alkoxy, haloalkoxy, alkenyl, alkynyl or alkylamino radical of 1 to 20 carbon atoms (for example of 5 to 20 carbon atoms, of 8 to 20 carbon atoms, of 9 to 20 carbon atoms, of 10 to 18 carbon atoms, of 12 to 18 carbon atoms, of 13 to 18 carbon atoms, of 14 to 18 carbon atoms, of 13 to 17 carbon atoms); or each R1 is independently selected from fluoro, chloro, bromo, iodo, hydroxy, oxyalkyl, amino, aminoalkyl or aminodialkyl radical; and n is any integer from 1 to m,

Abstract: This invention relates to potent selective agonists of the EP4 subtype of prostaglandin E2 receptors, their use or a formulation thereof in the treatment of glaucoma and other conditions, which are related to elevated intraocular pressure in the eye of a patient. This invention further relates to the use of the compounds of this invention for mediating the bone modeling and remodeling processes of the osteoblasts and osteoclasts.