Patent classifications
C07C391/00
Natural product-based synthesis of novel anti-infective isothiocyanate- and isoselenocyanate-functionalized amphilectane diterpenes
The marine natural product ()-8,15-diisocyano-11(20)-amphilectene, isolated from the Caribbean sponge Svenzea flava, was used as scaffold to synthesize five new products, all of which were tested against laboratory strains of Plasmodium falciparum and Mycobacterium tuberculosis H.sub.37Rv. The scaffold contains two isocyanide units that are amenable to chemical manipulation, enabling them to be elaborated into a small library of sulfur and selenium compounds. The scaffold along with its isothio- and isoselenocyanate analogs has low to sub-micro molar antiplasmodial activity.
NOVEL COMPOUND FOR LIGHT EMITTING DEVICE AND ORGANIC LIGHT EMITTING DEVICE INCLUDING SAME
A novel compound for a light emitting device, and an organic light emitting device containing the same are disclosed. The compound for a light emitting device is represented by Formula 1 below:
##STR00001##
Method of making complex nano particles and using the same to reduce cell viability
The development of anticancer metal-based drugs was done by reacting oyelamine with selenous acid to produce a quaternary ammonium salt which consequently converted to platinum and cobalt cationic complexes via complexing the first compounds with platinum (II) or cobalt (II) ions. The surface properties studies that were conducted included critical micelle concentration (CMC), maximum surface excess (max) and minimum surface area (Amin). Free energy of micellization (G mic) and adsorption (G ads) were calculated. Antitumor activities were tested by using Ehrlich Acites Carcinoma (EAC) as a model system of mice cell tumor. These compounds were also tested in vitro on human five monolayer tumor cell lines: MCF7 (Breast carcinoma), HEPG2 (liver carcinoma), and HCT116 (colon carcinoma), etc. FTIR spectra, elemental analysis and H1 NMR spectrum were performed to insure the purity of the prepared compounds.
Method of making complex nano particles and using the same to reduce cell viability
The development of anticancer metal-based drugs was done by reacting oyelamine with selenous acid to produce a quaternary ammonium salt which consequently converted to platinum and cobalt cationic complexes via complexing the first compounds with platinum (II) or cobalt (II) ions. The surface properties studies that were conducted included critical micelle concentration (CMC), maximum surface excess (max) and minimum surface area (Amin). Free energy of micellization (G mic) and adsorption (G ads) were calculated. Antitumor activities were tested by using Ehrlich Acites Carcinoma (EAC) as a model system of mice cell tumor. These compounds were also tested in vitro on human five monolayer tumor cell lines: MCF7 (Breast carcinoma), HEPG2 (liver carcinoma), and HCT116 (colon carcinoma), etc. FTIR spectra, elemental analysis and H1 NMR spectrum were performed to insure the purity of the prepared compounds.
Lipid-like nanocomplexes and uses thereof
Disclosed are compounds of formula (I) below: ##STR00001## wherein each of the variables A, B, X, W, V, R.sub.1-R.sub.5, and m is defined herein. Also disclosed are pharmaceutical compositions containing a nanocomplex, wherein the nanocomplex is formed of one of the compounds, and a protein, a nucleic acid, or a small molecule; and methods of treating a medical condition with one of the pharmaceutical compositions.
IDO/TDO inhibitor
A compound of formula (I) given below or a pharmaceutically acceptable salt of the compound is useful as an IDO/TDO inhibitor. Thus, the compound of formula (I) or the pharmaceutically acceptable salt of the compound can be used as, for example, a therapeutic agent for a disease or a disorder selected from tumor, infectious disease, neurodegenerative disorder, cataract, organ transplant rejection, autoimmune disease, postoperative cognitive impairment, and disease related to women's reproductive health [in the following formula (I), ring A represents an aromatic ring, an aliphatic ring, a heterocyclic ring, or a condensed ring of two or more rings selected from an aromatic ring, an aliphatic ring and a heterocyclic ring; X, R.sup.1 and R.sup.2 represent a substituent on a ring atom constituting ring A; m represents an integer of 0 to 6; X represents, for example, a halogen atom; and R.sup.1 and R.sup.2 are the same or different and are selected from, for example, the group consisting of groups of formula (a) or formula (b); and in the following formula (a) and formula (b), Y is selected from the group consisting of O, S, and Se, Z is selected from the group consisting of O, S, and Se, n represents an integer of 1 to 8, r represents an integer of 1 to 8, s represents an integer of 1 to 8, R.sup.4 represents, for example, C(NH)HN.sub.2, and R.sup.6 represents, for example, a substituted or unsubstituted aryl group]. ##STR00001##
IDO/TDO inhibitor
A compound of formula (I) given below or a pharmaceutically acceptable salt of the compound is useful as an IDO/TDO inhibitor. Thus, the compound of formula (I) or the pharmaceutically acceptable salt of the compound can be used as, for example, a therapeutic agent for a disease or a disorder selected from tumor, infectious disease, neurodegenerative disorder, cataract, organ transplant rejection, autoimmune disease, postoperative cognitive impairment, and disease related to women's reproductive health [in the following formula (I), ring A represents an aromatic ring, an aliphatic ring, a heterocyclic ring, or a condensed ring of two or more rings selected from an aromatic ring, an aliphatic ring and a heterocyclic ring; X, R.sup.1 and R.sup.2 represent a substituent on a ring atom constituting ring A; m represents an integer of 0 to 6; X represents, for example, a halogen atom; and R.sup.1 and R.sup.2 are the same or different and are selected from, for example, the group consisting of groups of formula (a) or formula (b); and in the following formula (a) and formula (b), Y is selected from the group consisting of O, S, and Se, Z is selected from the group consisting of O, S, and Se, n represents an integer of 1 to 8, r represents an integer of 1 to 8, s represents an integer of 1 to 8, R.sup.4 represents, for example, C(NH)HN.sub.2, and R.sup.6 represents, for example, a substituted or unsubstituted aryl group]. ##STR00001##
Complexes of diphenyl selenoxides, use thereof and catalysis methods
Novel complexes of diphenyl selenoxides and also use thereof and methods in which the complexes are used.
SULFONAMIDE DERIVATIVES AND THEIR USE AS SOLUBLE EPOXIDE HYDROLASE INHIBITORS
The present invention relates to compounds of formulae I and II. The compounds are useful for treating hypertension, atherosclerosis, pulmonary diseases, diabetes, pain, fibrosis, addictive disorders, inflammation, and immunological disorders or a condition treatable or preventable by inhibition of soluble epoxide hydrolase. Preferred compounds are N-((adamantan-1-yl)carbamoyl)-benzenesulfonamide derivatives. Exemplary compounds are e.g. N(((1r,3s,5R,7S)-3-hydroxyadamantan-1-yl)carbamoyl)-4-methylbenzenesulfonamide (example 14, compound 4a) 4-(tert-butyl)-N(((1r,3s,5R,7S)-3-hydroxyadamantan-1-yl)carbamoyl)benzenesulfonamide (example 15, compound 4b) N(((1r,3s,5R,7S)-3-hydroxyadamantan-1-yl)carbamoyl)-4-(trifluoromethyl)benzenesulfonamide (example 16, compound 4j). The present description discloses the synthesis and characterisation of exemplary compounds as well as pharmacological data thereof.
##STR00001##
NOVEL ORGANOSELENIUM COMPOUNDS, METHOD FOR PRODUCING SAME, AND PHARMACEUTICAL USES THEREOF IN PARTICULAR AS ANTITUMOR AGENTS
The invention relates to a selenium compound. Said selenium compound has formula (I), where R.sup.1=alkyl; R.sup.2=H, R.sup.4C(=0), R.sup.4OC(=0), a-aminoacyl, CH.sub.3SeCH.sub.2CH.sub.2CH(NH.sub.2)C(=0), CH.sub.3SeCH.sub.2CH.sub.2CH(OH)C(=0); X=OH, OR.sup.3, NH.sub.2, NR.sup.4R.sup.5, -amino acid, CH.sub.3SeCH.sub.2CH.sub.2CH(COOH)NH, CH.sub.3SeCH.sub.2CH.sub.2CH(COOH)0-; R.sup.3=alkyl; R.sup.4=alkyl, aryl; R.sup.5=H, alkyl, aryl; R.sup.4 and R.sup.5 which can together form a 5- or 6-membered cycloalkyl radical which can comprise a heteroatom; provided that when X=NH-terbutyl, R.sup.2C(=0)CH.sub.3. Said compound can be used as a pharmaceutical substance, in particular as an antitumour substance.