Abstract: Compounds of formula I, in which X1, X2, Sp, and R are as defined herein, are suitable for use in liquid-crystal media, such as liquid-crystal media used in liquid-crystal displays.

Abstract: The invention provides compositions of novel high penetration compositions (HPC) or high penetration prodrugs (HPP) for treatment of pulmonary conditions (e.g. asthma). The HPCs/HPPs are capable of being converted to parent active drugs or drug metabolites after crossing the biological barrier and thus can render treatments for the conditions that the parent drugs or metabolites can. Additionally, the HPPs are capable of reaching areas that parent drugs may not be able to access or to render a sufficient concentration at the target areas and therefore render novel treatments. The HPCs/HPPs can be administered to a subject through various administration routes, e.g., locally delivered to an action site of a condition with a high concentration or systematically administered to a biological subject and enter the general circulation with a faster rate.

Abstract: The invention provides crystalline forms of biphenyl-2-ylcarbamic acid 1-(2-{[4-(4-carbamoylpiperidin-1-ylmethyl)benzoyl]methylamino}ethyl)piperidin-4-yl ester, and pharmaceutically acceptable solvates thereof. The crystalline form can be a freebase, or a salt such as a diphosphate, monosulfate or dioxalate salt. The invention also provides pharmaceutical compositions comprising these crystalline compounds or prepared using these compounds; processes and intermediates for preparing the crystalline compounds; and methods of using these compounds to treat a pulmonary disorder.

Abstract: Amine functional polyamides comprise amine and ammonium groups along the polymer chain. Amine functional polyamides can be used as pharmaceutical agents and in pharmaceutical compositions. The amine functional polyamides are particularly useful in the treatment or prevention of mucositis and infection, specifically oral mucositis, surgical site infection, and lung infection associated with cystic fibrosis.

Abstract: Provided herein are arylsulfonamides that are useful for modulating CCR3 activity, and pharmaceutical compositions thereof. Also provided herein are methods of their use for treating, preventing, or ameliorating one or more symptoms of a CCR3-mediated disorder, disease, or condition.

Abstract: The invention provides crystalline forms of biphenyl-2-ylcarbamic acid 1-(2-{[4-(4-carbamoylpiperidin-1-ylmethyl)benzoyl]methylamino}ethyl)piperidin-4-yl ester, and pharmaceutically acceptable solvates thereof. The crystalline form can be a freebase, or a salt such as a diphosphate, monosulfate or dioxalate salt. The invention also provides pharmaceutical compositions comprising these crystalline compounds or prepared using these compounds; processes and intermediates for preparing the crystalline compounds; and methods of using these compounds to treat a pulmonary disorder.

Abstract: The invention provides compounds that are effective as inhibitors of human plasmin and plasma kallikrein, and that are useful for the prevention of blood loss and as components of fibrin adhesives. The invention further provides methods of making and using the compounds.

Abstract: A pharmaceutically-active polymeric compound of the general formula (I), Y-[Yn-LINK B-X]m-LINK B??(I) wherein (i) X is a coupled biological coupling agent of the general formula (II) Bio-LINK A-Bio??(II) wherein Bio is a biologically active agent fragment or precursor thereof linked to LINK A through a hydrolysable covalent bond; and LINK A is a coupled central flexible linear first segment of <2000 theoretical molecular weight linked to each of said Bio fragments; (ii) Y is LINK B-OLIGO; wherein (a) LINK B is a coupled second segment linking one OLIGO to another OLIGO and an OLIGO to X or precursor thereof; and (b) OLIGO is a short length of polymer segment having a molecular weight of less than 5,000 and comprising less than 100 monomeric repeating units; (iii) m is 1-40; and (iv) n is selected from 2-50. The compounds are useful as biomaterials, particularly, providing antibacterial activity in vivo.

Abstract: The present disclosure relates to new DNA-directed alkylating agents and water-soluble N-mustard agents with improved chemical stability and anti-tumor therapeutic efficacy.

Abstract: An intermediate of the formula (I) wherein the radicals R1 are independently of one another methyl, ethyl or n-propyl, is suitable for preparing a compound of the formula (A) wherein X is a group of the formula (A-I) or (A-II), Y is C11-C17alkyl, and Z is a direct bond, —(CH2)8— or —CH2—S—CH2—. The compounds of the formula (A) are useful for stabilizing an organic material against thermal, oxidative or light induced degradation.

Abstract: The invention provides crystalline forms of biphenyl-2-ylcarbamic acid 1-(2-{[4-(4-carbamoylpiperidin-1-ylmethyl)benzoyl]methylamino}ethyl)piperidin-4-yl ester, and pharmaceutically acceptable solvates thereof. The crystalline form can be a freebase, or a salt such as a diphosphate, monosulfate or dioxalate salt. The invention also provides pharmaceutical compositions comprising these crystalline compounds or prepared using these compounds; processes and intermediates for preparing the crystalline compounds; and methods of using these compounds to treat a pulmonary disorder.

Abstract: The invention relates to benzimidazole-carboxamide 5-HT4 receptor agonist compounds of formula (I) wherein R1 and X are as defined in the specification, or a pharmaceutically acceptable salt or solvate or stereoisomer thereof. The invention also relates to pharmaceutical compositions comprising such compounds, methods of using such compounds to treat diseases associated with 5-HT4 receptor activity, and processes and intermediates useful for preparing such compounds.

Abstract: A compound of the formula (A) wherein the radicals R1 are independently of one another methyl, ethyl or n-propyl, and X is C2-C8alkylene or C2-C8alkylene interrupted by sulfur, is useful for stabilizing an organic material against degradation induced by light, heat or oxidation.

Abstract: Method for producing 4-formylaminopiperidine derivatives of the formula (I) and also the acid addition salts of these compounds, comprising the reaction of 4-aminopiperidine derivatives of the formula (II) or the acid addition salts of these compounds in the presence of compounds of the formula (III) and the use of 4-formylaminopiperidine derivatives of the formula (I) produced in such a way for protecting inanimate organic material against the effect of light.

Abstract: Disclosed are compounds of the formula or a pharmaceutically acceptable salt or solvate thereof, wherein R1 is R is —C(O)—N(R27)(R28) or and the remaining variables are as defined in the specification. Also disclosed are pharmaceutical compositions comprising the compounds of formula I. Also disclosed are methods of treating cognitive or neurodegenerative diseases such as Alzheimer's disease. Also disclosed are pharmaceutical compositions and methods of treating cognitive or neurodegenerative diseases comprising the compounds of formula I in combination with a ?-secretase inhibitor other than those of formula I, an HMG-CoA reductase inhibitor, a gamma-secretase inhibitor, a non-steroidal anti-inflammatory agent, an N-methyl-D-aspartate receptor antagonist, a cholinesterase inhibitor or an anti-amyloid antibody.

Abstract: Hindered amines represented by the general formula (I): (wherein R is an alkyl or hydroxyalkyl group having 1 to 30 carbon atoms or alkenyl having 2 to 30 carbon atoms; n is an integer of 1 to 4; when n is 1, R1 is alkyl having 1 to 22 carbon atoms, alkenyl having 2 to 22 carbon atoms, or a group represented by the general formula (III): (R is as defined above), while when n is 2 to 4, R1 is an n-valent organic group having 2 to 20 carbon atoms). When added to synthetic resins or coating materials, the amines can impart long-period stabilizing effect to the resins or the materials and exhibit excellent resistance to extraction with acid rain or chemicals.

Abstract: The present invention provides a compound of a formula (I): wherein the variables are defined herein; to a process for preparing such a compound; and to the use of such a compound in the treatment of a chemokine (such as CCR3) mediated disease state.

Abstract: The invention provides crystalline forms of biphenyl-2-ylcarbamic acid 1-(2-{[4-(4-carbamoylpiperidin-1-ylmethyl)benzoyl]methylamino}ethyl)piperidin-4-yl ester, and pharmaceutically acceptable solvates thereof. The crystalline form can be a freebase, or a salt such as a diphosphate, monosulfate or dioxalate salt. The invention also provides pharmaceutical compositions comprising these crystalline compounds or prepared using these compounds; processes and intermediates for preparing the crystalline compounds; and methods of using these compounds to treat a pulmonary disorder.

Abstract: A subject of the present application is new derivatives of 4-aminopiperidines of formula in which R1, R2 and R3 represent various radical, and their preparation processes by synthetic methods in parallel in liquid and solid phase. These products having a good affinity with certain sub-types of somatostatin receptors, they are particularly useful for treating the pathological states or diseases in which one (or more) somatostatin receptors are involved.

Abstract: To provide a resist polymer comprising, as a structural unit, an acid-decomposable unit having a structure represented by formula (1) or (2) which exhibits a small line edge roughness and produces little defects in DUV excimer laser lithography or the like.

Abstract: Provided herein are arylsulfonamides that are useful for modulating CCR3 activity, and pharmaceutical compositions thereof. Also provided herein are methods of their use for treating, preventing, or ameliorating one or more symptoms of a CCR3-mediated disorder, disease, or condition.

Abstract: The present invention relates to the use of sterically hindered amines comprising one or more groups of the general formula (I) to stabilize inanimate organic material, more particularly plastics or coating materials, where R1 and R2 each independently, alike or different, are H, C1-C20 alkyl, C3-C15 cycloalkyl, aryl, hetaryl or a heterocycle, R4, R5, R6, and R7 each independently, alike or different, are C1-C20 alkyl, or R4 and R6 or R5 and R7 together are a tetramethylene or pentamethylene group, and R3 is aryl or hetaryl. The invention further relates to methods of stabilizing inanimate organic material, especially plastics or coating materials. Additionally provided by the invention are selected sterically hindered amines comprising one or more groups of the general formula (I). Additionally provided by the invention are materials that comprise selected sterically hindered amines.

Abstract: Disclosed is a temperature- and pH-sensitive hydrogel composed of a poly(amidoamine) oligomer only. The hydrogel is prepared in a simple manner and is readily released from the body. Further disclosed are a method for preparing the hydrogel and a drug carrier using the hydrogel.

Abstract: Novel 3,4-disubstituted-4-aryl-piperidine compounds are disclosed. Pharmaceutical compositions containing the 3,4-disubstituted-4-aryl-piperidine compounds and methods of their pharmaceutical uses are also disclosed. The compounds disclosed are useful, inter alia, as antagonists of opioid receptors.

Abstract: New carboxyphenyl-glycylboronic acid transition-state analog inhibitors, representative of a class of compounds effective against class C ?-lactamase AmpC. The new compounds improve inhibition by over two-orders of magnitude compared to analogous glycylboronic acids, with Ki values as low as 1 nM.

Abstract: A subject of the present application is new derivatives of 4-aminopiperidines of formula in which R1, R2 and R3 represent various radical, and their preparation processes by synthetic methods in parallel in liquid and solid phase. These products having a good affinity with certain sub-types of somatostatin receptors, they are particularly useful for treating the pathological states or diseases in which one (or more) somatostatin receptors are involved.

Abstract: The present invention relates to new non-peptide derivatives of formula (I), wherein R1-R5, Q and Z are as defined in the claims, and optical antipodes or racemates and/or salts and/or hydrates and/or solvates thereof, which are selective antagonists of bradykinin B1, to processes for producing these compounds, to pharmacological compositions containing them and to their use in therapy or prevention of painful and inflammatory conditions.

Abstract: Methods of treating an SCD-mediated disease or condition in a mammal, preferably a human, are disclosed, wherein the methods comprise administering to a mammal in need thereof a compound of formula (I) where x, y, G, J, K, L, M, Q, W, V, R2, R3, R5, R5a, R6, R6a, R7, R7a, R8 and R8a are defined herein. Pharmaceutical compositions comprising the compounds of formula (I) are also disclosed.

Abstract: The present invention provides highly pure repaglinide substantially free of dimer impurity, and process for the preparation thereof. The present invention also relates to 2-ethoxy-N-[(1S)-3-methyl-1-[2-(1-piperidinyl)phenyl]butyl]-4-[2-[[(1S)-3-methyl-1-[2-(1-piperidinyl)phenyl]butyl]amino]-2-oxoethyl]benzamide, an impurity of repaglinide, and a process for preparing and isolating thereof. The present invention further relates to pharmaceutical compositions comprising solid particles of pure repaglinide substantially free of dimer impurity or pharmaceutically acceptable salts thereof, wherein 90 volume-percent of the particles (D90) have a size of less than about 400 microns. The present invention also provides an optical resolution method of racemic 3-methyl-1-(2-piperidino-phenyl)-1-butylamine and use thereof for the preparation of repaglinide.

Abstract: Disclosed are aspartic protease inhibitors represented by the following structural formula: and pharmaceutically acceptable salts thereof. These compounds are orally active and bind to aspartic proteases to inhibit their activity. They are useful in the treatment or amelioration of diseases associated with aspartic protease activity. The present invention is also directed to pharmaceutical compositions comprising a compound described herein or enantiomers, diastereomers, or salts thereof and a pharmaceutically acceptable carrier or excipient.

Abstract: The invention relates to benzimidazole-carboxamide 5-HT4 receptor agonist compounds of formula (I) wherein R1 and X are as defined in the specification, or a pharmaceutically acceptable salt or solvate or stereoisomer thereof. The invention also relates to pharmaceutical compositions comprising such compounds, methods of using such compounds to treat diseases associated with 5-HT4 receptor activity, and processes and intermediates useful for preparing such compounds.

Abstract: Method for producing 4-formylaminopiperidine derivatives of the formula (I) and also the acid addition salts of these compounds, comprising the reaction of 4-aminopiperidine derivatives of the formula (II) or the acid addition salts of these compounds in the presence of compounds of the formula (III) and the use of 4-formylaminopiperidine derivatives of the formula (I) produced in such a way for protecting inanimate organic material against the effect of light.

Abstract: The invention provides crystalline forms of biphenyl-2-ylcarbamic acid 1-(2-{[4-(4-carbamoylpiperidin-1-ylmethyl)benzoyl]methylamino}ethyl)piperidin-4-yl ester, and pharmaceutically acceptable solvates thereof. The crystalline form can be a freebase, or a salt such as a diphosphate, monosulfate or dioxalate salt. The invention also provides pharmaceutical compositions comprising these crystalline compounds or prepared using these compounds; processes and intermediates for preparing the crystalline compounds; and methods of using these compounds to treat a pulmonary disorder.

Abstract: The invention provides compounds of the general formula (I) which have activity as Hsp90 inhibitors.

Abstract: The present invention is directed to novel derivatives of gambogic acid and analogs thereof. The present invention also relates to the discovery that novel derivatives of gambogic acid are activators of caspases and inducers of apoptosis. Therefore, the activators of caspases and inducers of apoptosis of this invention can be used to induce cell death in a variety of clinical conditions in which uncontrolled growth and spread of abnormal cells occurs.

Abstract: The present invention is directed to piperidine compounds that inhibit the glycine transporter GlyT1 and which are useful in the treatment of neurological and psychiatric disorders associated with glycinergic or glutamatergic neurotransmission dysfunction and diseases in which the glycine transporter GlyT1 is involved.

Abstract: An series of 2,7-disubstituted anthraquinone derivatives including a formula I are provided. R is a first substituted group selected from a group consisting of a hydrogen, an amino group, a nitro group, a hydroxyl group, a C1-C12 alkyl group, a C1-C12 alkyl halide group (—(CH2)nX), a C3-C12 cycloalkyl group, a benzyl group, a C1-C12 alkylamino group, a C5-C12 nitrocycloalkyl group and a heterocyclic group, n satisfies 1?n?12 and X is an atom selected from a group consisting of a fluoride (F), a chloride (Cl), a bromide (Br) and an iodine (I). The preparation method of the 2,7-disubstituted anthraquinone derivatives includes the steps of acetylating 2,7-diaminoanthraquinone to be one 2,7-disubstituted anthraquinone derivative, which can be further aminated to be another 2,7-disubstituted anthraquinone derivative.

Abstract: Processes and intermediates for preparing substituted 4-amino-1-(pyridylmethyl)-piperidine and related compounds in high yield and high purity are described. The substituted 4-amino-1-(pyridylmethyl)piperidine and related compounds prepared by the described processes are useful as muscarinic receptor antagonists.

Abstract: This invention provides compounds of formula I: wherein a, b, c, d, m, n, p, s, t, Ar1, R1, R2, R3, R4, R6, R7, R8, and W are as defined in the specification. The compounds of formula I are mescaline receptor antagonists. The invention also provides pharmaceutical compositions containing such compounds, processes and intermediates for preparing such compounds and methods of using such compounds to treat pulmonary disorders.

Abstract: The invention describes novel compound of the formula I, wherein the general symbols are as defined in claim 1, as stabilizers for protecting organic materials, in particular synthetic polymers, against oxidative, thermal, dynamic, light-induced and/or ozone-induced degradation.

Abstract: Disclosed herein are compounds of Formula I, or a pharmaceutically acceptable salt, amide, ester, or prodrug thereof. Also disclosed are methods of inhibiting an activity of a monoamine receptor comprising contacting the monoamine receptor or a system containing the monoamine receptor with an effective amount of one or more of the compounds of Formula I. Disclosed are also methods of inhibiting an activation of a monoamine receptor comprising contacting the monoamine receptor or a system containing the monoamine receptor with an effective amount of one or more of the compounds of Formula I. Furthermore, methods of treating psychotic disease using a compound of Formula I are disclosed.

Abstract: The present invention provides a compound of a formula (I): wherein the variables are defined herein; to a process for preparing such a compound; and to the use of such a compound in the treatment of a chemokine (such as CCR3) or H1 mediated disease state.

Abstract: This invention provides compounds of formula I: wherein a, b, c, d, m, n, p, r, R1, R2, R3, R4, R5, R6, R7, and W are as defined in the specification. The compounds of formula I are muscarinic receptor antagonists. The invention also provides pharmaceutical compositions containing such compounds, processes and intermediates for preparing such compounds and methods of using such compounds to treat pulmonary disorders.

Abstract: The invention provides compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with the activity of liver X receptors (LXRs).

Abstract: The present invention relates to compounds of formula (I): The variables recited in formula (I) are defined in the specification. The present invention also relates to processes of preparing compounds of formula (I) and uses of such compounds for treating a chemokine (e.g., CCR3) or H1 mediated disease state.

Abstract: This invention provides 4-amino-1-benzylpiperidine and related compounds and pharmaceutically acceptable salts thereof which are useful as muscarinic receptor antagonists. This invention also provides pharmaceutical compositions containing such compounds; processes and intermediates useful for preparing such compounds; and methods for treating disease conditions mediated by muscarinic receptors, such as overactive bladder, irritable bowel syndrome, asthma and chronic obstructive pulmonary disease, using such compounds.

Abstract: Processes and intermediates for preparing 2-substituted piperidines such as 2-substituted d-threo piperidines are provided, including processes and intermediates for resolution of piperidyl acetamide stereoisomers.

Abstract: Compounds of formula (I): wherein: when X is NR5, Y is absent or is CH2; when X is CH2, Y is absent, CH2, NR6, O, S, S(O) or S(O)2; Z is a 5- or 6-membered heterocyclyl ring; compositions comprising them, processes for preparing them and their use in medical therapy (for example modulating CCR5 receptor activity in a warm blooded animal).

Abstract: The present invention relates to novel pyridone derivatives capable of inhibiting ?4 integrin mediated cell adhesion, processes for their preparation, compositions comprising them and their use in the treatment of diseases capable of being modulated by the inhibition of cell adhesion.

Abstract: The present invention is related to novel processes for preparing anhydrous and hydrated forms of piperidine derivatives, polymorphs and pseudomorphs thereof of the formulas which are useful as antihistamines, antiallergic agents and bronchodilators.