Abstract: Uses of compound of Formula I: or pharmaceutically acceptable enantiomers, salts, solvates or prodrugs thereof are described. The compounds of Formula I are useful as IDO1 inhibitors. These are also useful for the treatment and/or prevention of cancer and endometriosis.

Abstract: The present invention relates to compounds of formula (I), and their pharmaceutically acceptable salts, solvates, hydrates, geometrical isomers, tautomers, optical isomers or N-oxides, which are inhibitors of SSAO activity. The invention further relates to pharmaceutical compositions comprising these compounds and to the use of these compounds for the treatment of medical conditions wherein inhibition of SSAO activity is beneficial, such as inflammatory diseases and immune disorders.

Abstract: Described herein, inter alia, are compositions and methods for treating or preventing hyperproliferative disorders, including cancer.

Abstract: A manufacturing method of an isocyanate compound including obtaining a reaction solution containing an aldehyde compound by reacting a compound represented by Formula (a1) or (a2) with hydrogen and carbon monoxide in the presence of a metal compound of groups 8 to 10 and a phosphorus compound, neutralizing the reaction solution, purifying an aldehyde compound by distilling the neutralized reaction solution, reacting the aldehyde compound with ammonia and with hydrogen in the presence of a catalyst to obtain an amine compound; and reacting the amine compound with a carbonylating agent to obtain an isocyanate compound, wherein the phosphorus compound is represented by the Formula (R1O)3P, and the base compound is at least one selected from carbonate and hydrogen carbonate of metals of group I and carbonate and hydrogen carbonate of metals of group II, wherein the neutralizing the reaction solution is performed within a temperature range of 40° C. to 50° C.

Abstract: The present invention relates to compounds of general formula I, wherein D1 to D3, A, R1, R2, Y and n are defined as in claim 1, which have valuable pharmacological properties, in particular are inhibitors of plasma kallikrein. The compounds are suitable for treatment and prevention of diseases which can be influenced by influenced by inhibition of plasma kallikrein, such as diabetic complications, particularly in the treatment of retinal vascular permeability associated with diabetic retinopathy and diabetic macular edema.

Abstract: A manufacturing method of an amine compound including obtaining a reaction solution containing an aldehyde compound by reacting a compound represented by Formula (a1) or (a2) with hydrogen and carbon monoxide in the presence of a metal compound of groups 8 to 10 and a phosphorus compound, neutralizing the reaction, purifying an aldehyde compound by distilling the neutralized reaction solution, and reacting the aldehyde compound with ammonia and with hydrogen in the presence of a catalyst to obtain an amine compound, wherein the phosphorus compound is represented by the Formula (R1O)3P, and the base compound is at least one selected from carbonate and hydrogen carbonate of metals of group I and carbonate and hydrogen carbonate of metals of group II, and wherein the neutralizing the reaction solution is performed within a temperature range of 40° C. to 50° C.

Abstract: Inhibitors of HBV replication of Formula (I) including stereochemically isomeric forms, and salts, hydrates, solvates thereof, wherein X, R1, R2, R3 and R4 have the meaning as defined herein. The present invention also relates to processes for preparing said compounds, pharmaceutical compositions containing them and their use, alone or in combination with other HBV inhibitors, in HBV therapy.

Abstract: The present invention relates to a process for preparing compound 1 that is useful as an antifungal agent. In particular, the invention seeks to provide new methodology for preparing compound 1 and substituted derivatives thereof.

Abstract: The present invention provides compounds comprising fused tricyclic backbone structure and processes for their preparation. The invention further provides compounds and compositions useful in the treatment of pain and any type of disorder or symptom associated therewith.

Abstract: Provided are a compound represented by Formula 1, and an organic electric element comprising a first electrode, a second electrode, and an organic material layer formed between the first electrode and the second electrode, wherein the organic material layer comprised the compound represented by Formula 1, and the driving voltage of an organic electronic device can be lowered, and the luminous efficiency, color purity and life time of an organic electronic device can be improved by comprising the compound represented by Formula 1 in the organic material layer.

Abstract: The present invention is directed to certain amides and heterocyclic compounds. The present invention also relates to uses of these compounds to treat several diseases including autoimmune disorders, cardiovascular disorders, inflammation, central nervous system disorders, arterial thrombotic disorders, fibrotic disorders, glaucoma, and neoplastic disorders.

Abstract: The present invention relates to an improved process for the preparation of Daclatasvir dihydrochloride by using compound salt of formula (VIIc).

Abstract: Disclosed are small molecule therapeutic compounds that are potent inhibitors of arginase 1 and arginase 2 activity. Also disclosed are pharmaceutical compositions comprising the compounds, and methods for using the compounds for treating or preventing a disease or condition associated with arginase activity.

Abstract: The present invention relates to novel compounds and methods for the manufacture of inhibitors of deubiquitylating enzymes (DUBs). In particular, the invention relates to the inhibition of ubiquitin C-terminal hydrolase L1 (UCHL1). The invention further relates to the use of DUB inhibitors in the treatment of cancer and other indications. Compounds of the invention include compounds having the formula (I) or a pharmaceutically acceptable salt thereof, wherein R1 to R8 are as defined herein.

Abstract: The present invention provides novel derivative of ?-lactam antibiotics, such as meropenem. The inventive compounds include compounds of Formula (I), and pharmaceutically acceptable salts, solvates, hydrates, polymorphs, co-crystals, tautomers, stereoisomers, isotopically labeled derivatives, and prodrugs thereof. Also provided are particles (e.g., nanoparticles) and pharmaceutical compositions thereof that are mucus penetrating. The inventive particles and pharmaceutical compositions may be useful in delivering an inventive compound to the respiratory tract of a subject. The invention further provides methods of using and kits including the inventive compounds, particles thereof, and/or pharmaceutical compositions thereof for treating and/or preventing a pulmonary disease (e.g., a respiratory tract infection).

Abstract: The present invention is concerned with substituted oxazole derivatives that selectively modulate, regulate, and/or inhibit signal transduction mediated by certain native and/or mutant protein kinases implicated in a variety of human and animal diseases such as cell proliferative, metabolic, autoimmune, allergic, hematological, inflammatory and degenerative disorders. In particular, the compounds of the invention are Syk inhibitors. The invention also relates to a process for manufacturing the compounds of the invention.

Abstract: The present disclosure is directed to compounds of formula (I), and pharmaceutically acceptable salts thereof, as mPGES-1 inhibitors. These compounds are inhibitors of the microsomal prostaglandin E synthase-1 (mPGES-1) enzyme and are therefore useful in the treatment of pain and/or inflammation from a variety of diseases or conditions, such as asthma, osteoarthritis, rheumatoid arthritis, acute or chronic pain and neurodegenerative diseases.

Abstract: The present invention is directed to pyrimidine carboxamide compounds of formula I which are useful as therapeutic agents for the treatment of central nervous system disorders associated with phosphodiesterase 2 (PDE2). The present invention also relates to the use of such compounds for treating neurological and psychiatric disorders, such as schizophrenia, psychosis, Parkinson's disease, Parkinson's disease dementia (PDD), or Huntington's disease, and those associated with striatal hypofunction or basal ganglia dysfunction.

Abstract: Compounds of Formula II, wherein X is selected from chloro, fluoro, bromo and iodo, R1 and R2 are each independently selected from H, —CH3, —CH2CH3, —CH2CH2CH3, or —CH(CH3)2; compositions containing them, their use in therapy, including their use as anti-mycobacterial agents, for example in the treatment of a mycobacterial infection in a mammal, and methods for the preparation of such compounds, are provided.

Abstract: Provided is a method for resolution of formula 4-[4-dimethylamino-1-(4-fluorophenyl)-1-hydroxylbutyl]-3-hydroxy-methyl benzonitrile as an enantiomer thereof, comprising the following steps: a salt of (S)-4-[4-dimethylamino-1-(4-fluorophenyl)-1-hydroxylbutyl]-3-hydroxymethyl benzonitrile with a resolving agent D-(+)di-p-toluoyl tartaric acid was crystallized in a resolving solvent; the method is characterized in that the resolving solvent is an ether solvent. Also provided is a new crystal form of the resolved intermediate.