Abstract: Combined apparatus (1) for the synthesis of urea from ammonia and carbon dioxide, comprising an internal wall (3) which delimits two coaxial zones (4) inside the apparatus, operating respectively as reaction (4) and condensation (5) zones, and optionally also comprising a stripping zone and/or a scrubber integrated in the same apparatus.

Abstract: There are disclosed compounds that modulate or inhibit the enzymatic activity of indoleamine 2,3-dioxygenase (IDO), pharmaceutical compositions containing said compounds and methods of treating proliferative disorders, such as cancer, viral infections and/or inflammatory disorders utilizing the compounds of the invention.

Abstract: The present invention relates to a compound represented by the general formula (A), a base- and/or radical-generating agent comprising the compound, and so on.

Abstract: In certain embodiments, the disclosure relates to methods of treating or preventing a PGAM1 mediated condition such as cancer or tumor growth comprising administering an effective amount of PGAM1 inhibitor, for example, an anthracene-9,10-dione derivative to a subject in need thereof. In certain embodiments, the disclosure relates to methods of treating or preventing cancer, such as lung cancer, head and neck cancer, and leukemia, comprising administering a therapeutically effective amount of a pharmaceutical composition comprising a compound disclosed herein or pharmaceutically acceptable salt to a subject in need thereof.

Abstract: The subject of the invention is a process for the preparation of Latanoprostene bunod of formula (I) with a purity higher than 95% where chromatography is used applying normal phase gravity silica gel column chromatography where the used silica gel is irregular silica gel or spherical silica gel an as eluent and eluent mixture consisting of an apolar and a polar solvent is used and if desired, contamination of the purified compound of formula I arising from the solvents are removed by silica gel filtration chromatography.

Abstract: Inhibitors of HBV replication of formula (I) including stereochemically isomeric forms, and salts, hydrates, solvates thereof, wherein X, R1 to R7 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: Object of the present invention is an improved process for the preparation of (3R,4R)-1-benzyl-4-methylpiperidin-3-amine by means of chiral Rhodium catalysts.

Abstract: An oligo-guanidine as cell penetrating agents/carriers includes a heterocyclic ring including 4-aminopiperidine, piperazine, morpholine having at least one N-terminal based heterocyclic ring or at least one O-heteroatom based heterocyclic ring tailored with hydrophobic and/or lipophilic group. The oligo-guanidine is adapted as an effective molecular transporter to transport and/or delivery therapeutics, therapeutic candidates, probes, or other molecules of interest across biological barriers including oligonucleotides. Advantageously, the oligo-guanidine is capable of being internalized into cells (in-vitro and in-vivo) with enhanced cellular uptake in nanomolar concentration.

Abstract: The present application relates to novel substituted N,2-diarylquinoline-4-carboxamide derivatives, to processes for preparation thereof, to the use thereof alone or in combinations for treatment and/or prevention of diseases, and to the use thereof for production of medicaments for treatment and/or prevention of diseases, especially for treatment and/or prevention of fibrotic and/or inflammatory disorders.

Abstract: Provided herein are molecules and salts thereof, arrays containing molecules and salts thereof, solid supports containing molecules and salts thereof, kits containing molecules or salts thereof, and methods of determining alignment of photolithographic masks comprising molecules or salts thereof.

Abstract: The synthesis and in vitro and in vivo anti-breast and anti-prostate cancers activities of novel C-4 heteroaryl 13-cis retinamides that modulate Mnk-eIF4E and AR signaling are discussed. In both breast and prostate cancer cell lines, these compounds induce Mnk1/2 degradation to substantially suppress eIF4E phosphorylation. In prostate cancer cells, the compounds induce degradation of both full-length androgen receptor (fAR) and splice variant AR (AR-V7) to inhibit AR transcriptional activity. The consequences of these multiple activities resulted in inhibition of cell growth and migration and induction of apoptosis. Finally and importantly, the compounds demonstrate strong in vitro and in vivo anti-breast and anti-prostate cancer activities, with no apparent host toxicities.

Abstract: The present disclosure provides substituted pyrimidine compounds of Formula (I), and the pharmaceutically acceptable salts, prodrugs, and solvates thereof, wherein A1, X, A2, W1, W2, W3, E, Z, and R4 are defined as set forth in the specification. The present disclosure is also directed to the use of compounds of Formula (I) to treat a disorder responsive to the blockade of sodium channels. Compounds of the present disclosure are especially useful for treating pain.

Abstract: The disclosure provides compounds of the formula I and the pharmaceutically acceptable salts thereof. The variables, e.g. R1, R2, R3, R4, A, B, J, V, W, M, J and Ar are defined herein. The disclosure also provides pharmaceutical compositions comprising a compound or salt of formula I and a pharmaceutically acceptable carrier, methods of inhibiting dihydrofolate reductase (DHFR) in vitro or in vivo with a compound or salt of formula I, and methods of treating a bacterial infections, fungal infections, and protozoal infections with a compound or salt of formula I. A compound or salt of formula I can be the first and only active ingredient used in a pharmaceutical composition or method of this disclosure or may be combined with one or more additional active ingredients that are not compounds or salts of formula I.

Abstract: A problem of the present invention is to provide a new compound which has NK1 receptor antagonist activity, and thus is useful for the prevention or treatment of cancer-chemotherapy-induced nausea and vomiting. A compound represented by the formula (I): wherein W represents a fluorine atom and the like, ring A represents a cycloalkyl and the like, X1 represents CH or N, R represents methyl and the like, Y represents 0 to 2, U1, U2 and U3 each independently represents a single bond and the like, or a pharmaceutically acceptable salt thereof. The compounds of the present invention or pharmaceutically acceptable salts thereof have an excellent NK1 receptor antagonist activity, and thus are also useful as an agent for the prevention or treatment of cancer-chemotherapy-induced nausea and vomiting.

Abstract: Described are high energy light blocking compounds and ophthalmic devices containing the compounds. In particular, described are hydroxyphenyl naphthotriazole structures with polymerizable functionality that block high energy light and are visibly transparent. The hydroxyphenyl naphthotriazole structures can be incorporated into ophthalmic devices, such as hydrogel contact lenses, to protect eyes from high energy light radiation.

Abstract: In one aspect, the invention relates to a crystalline form of the structure: or a pharmaceutically acceptable salt thereof, having neprilysin inhibition activity. In another aspect, the invention relates to pharmaceutical compositions comprising this crystalline form; methods of using this crystalline form and its soluble form (I); and processes for preparing soluble (I) and crystalline (I?) forms.

Abstract: The present invention relates to compounds according to formula (I), which are suitable for use in electronic devices, preferably organic electroluminescent devices.

Abstract: This present application disclosed a series of selective adenylyl cyclase 1 (AC1) inhibitors as a pain therapeutic. Those compounds may provide an effective method of treatment for chronic/inflammatory pain. Those compounds may also prevent opioid dependence and/or reduce opioid dependence. Both method and composition matters are within the scope of this invention.

Abstract: A process for preparing, 1,1,3-Trioxo-1,2-benzothiazole-6-carboxamide of formula (I) comprising: reacting 2-chloro-sulfonyl-terephthalic acid dialkyl ester of formula (II) with ammonia (N H3) or ammonium containing-salt; wherein R represents a branched or non-branched C1-C12 alkyl.

Abstract: The present invention provides a process for preparation of the compound of formula (VI), wherein each symbol is as defined in the specification, without using any intermediate compound showing mutagenicity. The process comprises salt formation of the intermediate compound of formula (I) with acid to enable optical resolution to isolate the intermediate compound of formula (II) in a stereo-selective manner.

Abstract: Processes are disclosed for making vortioxetine and pharmaceutically acceptable salts thereof. A propylene glycol solvate of vortioxetine hydrobromide is disclosed. A novel crystalline form of vortioxetine hydrobromide propylene glycol solvate, designated form AC1, is disclosed along with a method for making same. Form AC1 may be characterized by an x-ray powder diffraction pattern with peaks at about 19.64, 22.85, 25.51, 29.57, 30.18±0.2 degrees 2-theta.

Abstract: A continuous process for the preparation of propylene oxide, comprising providing a liquid feed stream comprising propene, hydrogen peroxide, methanol, water, at least one dissolved potassium salt of hydroxyethylidenediphosphonic acid, and optionally propane; passing the liquid feed stream provided in (i) into an epoxidation reactor comprising a catalyst comprising a titanium zeolite of structure type MFI, and subjecting the liquid feed stream to epoxidation reaction conditions in the epoxidation reactor, obtaining a reaction mixture comprising propylene oxide, methanol, water, and the at least one dissolved potassium salt of hydroxyethylidenediphosphonic acid, and optionally propane; removing an effluent stream from the epoxidation reactor, the effluent stream comprising propylene oxide, methanol, water, at least a portion of the at least one potassium salt of hydroxyethylidenediphosphonic acid, and optionally propane.

Abstract: A process for preparing a batch of highly purified, pharmaceutical grade tasimelteon comprises analyzing a batch of tasimelteon synthesized under GMP conditions for the presence of one or more identified impurities.

Abstract: The present invention relates to the synthesis of intermediate compounds which can be used in the synthesis of mint lactone and related compounds, including 3,6-dimethylhexahydrobenzofuran-2-ones, isomers, and other derivatives.

Abstract: The present disclosure relates to C-glycoside derivatives having a fused phenyl ring or pharmaceutical acceptable salts thereof, a method for preparing the same, a pharmaceutical composition comprising the same, a use thereof and a method for dual inhibition of SGLT1 and SGLT2 using the same. A novel compound of the present disclosure has a dual inhibitory activity against SGLT1 and SGLT2, thus being valuably used as a diabetes therapeutic agent.

Abstract: Newly synthesized derivatives of BAS00127538 have been discovered to possess antibiotic activity and to combat resistant bacterial strains. Compounds and pharmaceutical compositions containing these compounds are described, and are based on a generic scaffold structure. Synthetic methods and methods of using the compounds also are described. Preferred compound 6jc48-1 ((E)-2,4-bis(4-bromophenyl)-6-(4-(dimethyl-amino)styryl)pyrylium boron tetrafluoride salt) binds to Lipid II with high affinity, has markedly reduced cytotoxicity than BAS00127538, and retains activity against drug-resistant strains of Enterococci. It is stable in plasma, has dramatically improved pharmacokinetic and pharmacodynamics properties, and possesses in vivo efficacy in a mouse model of sepsis.

Abstract: Disclosed is a configurational stereoisomer, referred to as enantiomer E4, of flocoumafen, the enantiomer E4 having, as determined by the chromatographic analysis of flocoumafen including four configurational stereoisomers of flocoumafen, carried out under conditions described hereinafter, a retention time t4 with a value such that t1<t2<t3<t4; t1, t2 and t3 representing the retention times of the configurational stereoisomers of flocoumafen different from the enantiomer E4, the analysis being carried out at a temperature of 23.5° C.

Abstract: The invention discloses novel processes for production, enrichment and/or isolation of alpha-tocotrienol from source material comprising at least one non-alpha-tocotrienol, such as natural extracts comprising mixed tocotrienols.

Abstract: The present invention relates to xanthone analogs. Such compounds may be used in the treatment of bacterial infections.

Abstract: The invention relates to a liquid-crystalline medium, preferably having a nematic phase and dielectric anisotropy of 0.5 or more, which comprises one or more compounds of formula S in which denotes and to the use thereof in an electro-optical display, particularly in an active-matrix display based on the IPS or FFS effect, to displays of this type which contain a liquid-crystalline medium of this type, and to the use of the compounds of formula S for the improvement of the transmission and/or response times of a liquid-crystalline medium which comprises one or more additional mesogenic compounds.

Abstract: Described herein are compounds that are somatostatin modulators, methods of making such compounds, pharmaceutical compositions and medicaments comprising such compounds, and methods of using such compounds in the treatment of conditions, diseases, or disorders that would benefit from modulation of somatostatin activity.

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 or prevention of mGluR5 mediated disorders, such as acute and/or chronic neurological disorders, cognitive disorders and memory deficits, as well as acute and chronic pain.

Abstract: The invention relates to quinazoline derivatives of formula (I), wherein m is an integer from 1 to 3; R? represents halogeno or C1-3alkyl; X1 represents —O—; R2 is selected from one of the following three groups: 1) C1-5alkylR3 (wherein R3 is piperidin-4-yl which may bear one or two substituents selected from hydroxy, halogeno, C1-4alkyl, C1-4hydroxyalkyl and C1-4alkoxy; 2) C2-5alkenylR3 (wherein R3 is as defined hereinbefore); 3) C2-5alkynylR3 (wherein R3 is as defined hereinbefore); and wherein any alkyl, alkenyl or alkynyl group may bear one or more substituents selected from hydroxy, halogeno and amino; and salts thereof; processes for their preparation, pharmaceutical compositions containing a compound of formula (I) or a pharmaceutically acceptable salt thereof as active ingredient. The compounds of formula (I) and the pharmaceutically acceptable salts thereof inhibit the effects of VEGF, a property of value in the treatment of a number of disease states including cancer and rheumatoid arthritis.

Abstract: The invention relates to Crystal form I, Crystal form II and Crystal form III of N-(4-((3-chloro-4-fluorophenyl)amino)-7-((7-methyl-7-azaspiro[3.5]nonan-2-yl)methoxy)quinazolin-6-yl)acrylamide represented by the following Formula (I), and preparation methods thereof, wherein the Crystal form I has an X-ray powder diffraction pattern having characteristic peaks at the 20 positions of 6.7±0.2°, 7.9±0.2°, 8.6±0.2°, 12.0±0.2°, 13.9±0.2°, 15.9±0.2°, 17.3±0.2°, 18.3±0.2°, 18.7±0.2°, 21.0±0.2°, and 23.0±0.2°, as determined by using Cu-K? radiation; the Crystal form II has an X-ray powder diffraction pattern having characteristic peaks at the 20 positions of 6.9±0.2°, 8.5±0.2°, 14.8±0.2°, 15.6±0.2°, 16.7±0.2°, 17.1±0.2°, 17.9±0.2°, 18.7±0.2°, 19.1±0.2°, 21.5±0.2°, 23.5±0.2°, and 25.7±0.2°, as determined by using Cu-K? radiation; and the Crystal form III has an X-ray powder diffraction pattern having characteristic peaks at the 20 positions of 4.9±0.2°, 6.1±0.2°, 7.4±0.2°, 11.4±0.2°, 12.2±0.2°, 16.6±0.2°, and 18.4±0.

Abstract: The present invention relates a new process to synthesize 1-((4-(4-Fluoro-2-methyl-1H-indol-5-yloxy)-6-methoxyquinolin-7-yloxy)methyl)cyclopropanamine (AL3818). A stable crystalline form of Al3818 has been prepared. Salts and their crystalline forms of AL3818 have been also prepared. Anti-cancer and optometric activities of AL3818 and its salts have been further tested. New process has been outlined in Scheme I.

Abstract: Compounds of Formula (I): (Formula I), wherein Z1 is NR1A, CHR1A, CR1BR1B; one of Z2 and Z3 is CH or CR1A?, the other is N, CH or CR1A?; n is 0, 1 or 2; q is 0, 1 or 2; R1A, R1A?, R1B, R2, and R3 are as defined herein, their use as inhibitors of RSV and related aspects.

Abstract: Provided herein are heterocyclic derivative compounds and pharmaceutical compositions comprising said compounds that are useful for inhibiting plasma kallikrein. Furthermore, the subject compounds and compositions are useful for the treatment of diseases wherein the inhibition of plasma kallikrein inhibition has been implicated, such as angioedema and the like.

Abstract: The present invention provides a compound of formula (I) or a pharmaceutically acceptable salt thereof; a method for manufacturing the compounds of the invention, and its therapeutic uses. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.

Abstract: The present invention provides, in part, compounds of Formula I: and pharmaceutically acceptable salts thereof; processes for the preparation of; intermediates used in the preparation of; and compositions containing such compounds or salts, and their uses for treating D1-mediated (or D1-associated) disorders including, e.g., schizophrenia (e.g., its cognitive and negative symptoms), cognitive impairment (e.g., cognitive impairment associated with schizophrenia, AD, PD, or pharmacotherapy therapy), and Parkinson's disease.

Abstract: Provided is a synthesis method for a voriconazole intermediate condensate as shown in formula II or an acid addition salt thereof. As shown in reaction formula 1, the product is prepared via compounds III and IV. The synthesis method adjusts the feeding means, and the reaction conditions are mild and controllable, thereby reducing the production of impurity A, avoiding the use of highly toxic metal lead, and eliminating the risk of highly toxic metal remaining in a drug. The product has a higher purity and significant industrial application value.

Abstract: The present invention provides compounds of Formula (I): wherein all variables are as defined in the specification, and compositions comprising any of such novel compounds. These compounds are APJ agonists which may be used as medicaments.

Abstract: The present invention relates to a Rho-associated protein kinase inhibitor of Formula (I), a pharmaceutical composition comprising the same, a preparation method thereof, and use thereof for the prevention or treatment of a disease mediated by the Rho-associated protein kinase (ROCK).

Abstract: The present invention relates to substituted amide derivatives having dual pharmacological activity towards both the sigma (?) receptor, and the ?-opioid receptor, to processes of preparation of such compounds, to pharmaceutical compositions comprising them, and to their use in therapy, in particular for the treatment of pain.

Abstract: The present application relates to crystalline and amorphous Vilazodone hydrochloride. The present application further relates to amorphous solid dispersions of vilazodone hydrochloride with pharmaceutically acceptable carriers. The present application also relates to a process for the preparation of form I of vilazodone free base.

Abstract: The present disclosure provides efficient, economical, and improved processes for synthesizing lifitegrast and intermediates thereof. The currently discloses processes provide a direct synthetic route, avoiding protection or deprotection steps. The currently disclosed process also provides processes for synthesizing lifitegrast using a reduced number of synthetic steps.

Abstract: A method of treating cancer in a subject includes administering to the subject a therapeutically effective amount of a small molecule agonist of EphA2 receptor protein, the small molecule having a general formula: A-L-X-Z (I).

Abstract: The present invention is directed to new bifunctional compounds and methods for treating HIV infections. The bifunctional small molecules, generally referred to as ARM-HI's, function through orthogonal pathways, by inhibiting the gp120-CD4 interaction, and by recruiting anti-DNP antibodies to gp120-expressing cells, thereby preventing cell infection and spread of HIV. It has been shown that ARM-HI's bind to gp120 and gp-120 expressing cells competitively with CD4, thereby decreasing viral infectivity as shown by an MT-2 cell assay, the binding leading to formation of a ternary complex by recruiting anti-DNP antibodies to bind thereto, the antibodies present in the ternary complex promoting the complement-dependent destruction of the gp120-expressing cells. Compounds and methods are described herein.

Abstract: The invention generally relates to substituted benzofuranyl and substituted benzoxazolyl compounds, and more particularly to a compound represented by Structural Formula (I) or (II), or a pharmaceutically acceptable salt thereof, wherein the variables are as defined and described herein. The invention also includes the synthesis and use of a compound of Structural Formula A, or a pharmaceutically acceptable salt or composition thereof, e.g., in the treatment of cancer (e.g., mantle cell lymphoma), and other diseases and disorders.

Abstract: The present invention relates to an improved crystallization procedure to obtain canagliflozin hemihydrate crystals having a narrow particle size distribution by removing a small part of the crystalline suspension in the crystallization vessel from said vessel and subjecting said part to particle size reduction of the formed crystals followed by heating and reintroducting said part of the crystalline suspension again in the crystallization vessel which is kept within a specific temperature range.

Abstract: Among the various aspects of the present disclosure is the provision of a compositions for binding sphingosine-1-phosphate receptor 1 (S1P1), imaging of S1P1, and methods of use thereof. Provided are imaging agents for imaging S1P1 and S1P1 associated diseases, disorders, and conditions. Also provided are therapeutic compositions and methods for the treatment of S1P1 associated diseases, disorders, and conditions.