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Oxazolidine derivatives and pharmaceutically acceptable salts thereof

An oxazolidine derivative represented by the formula (I) STR1 wherein R1, R2 and R3 are H, optionally halogenated alkyl, optionally halogenated alkoxy, OH, halo, NO2, amino optionally having acetyl or alkyl, COOH, alkoxycarbonyl, CN, alkanoyl, 2-oxazolyl, or R1 and R2 may be combined with each other to represent –(CH2)p — or –O(CH2)q O– (p is 3-5, q is 1-3) to form a ring, m and n are each 0 or 1, R4 and R5 are H or alkyl, X is C or N, Y is CH2 OH, CHO or COOR6 (R6 is alkyl, benzyl or H), A is alkylene, carbonyl or sulfonyl, B is alkylene, E is alkylene which may be substituted with halo or is alkenylene, Z is O or S, except for a compound wherein n is 0, m is 1 and Y is CH2 OH, and except for a compound wherein n is 0, Y is COOR6 (R6 is alkyl), a salt thereof, a process for its preparation, anti-hyperlipidemic composition containing the derivative as an active ingredient and a method for treating hyperlipidemia comprising administering the derivative.

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Reference£º
Copper catalysis in organic synthesis – NCBI,
Special Issue “Fundamentals and Applications of Copper-Based Catalysts”

 

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Pyridine derived agents for cardiovascular diseases

STR1 Compounds of formula (I) or a biolabile ester thereof, or a pharmaceutically acceptable salt of either, wherein Rl, R2, R3 and R4 are each independently selected from H or C1 -C4 alkyl; R5 is (CH2)m SO2 R6, (CH2)m NHSO2 R6 or (CH2)m NHCOR7 ; R6 and R7 are C1 -C6 alkyl, C1 -C3 perfluoroalkyl(CH2)n, C3 -C6 cycloalkyl(CH2)n, aryl(CH2)n or heteroaryl(CH2)n ; or R6 is NR8 R9 ; R8 is H or C1 -C4 alkyl; R9 is C1 -C6 alkyl, C3 -C6 cycloalkyl(CH2)n, aryl(CH2)n or heteroaryl(CH2)n ; or R8 and R9 together with the nitrogen atom to which they are attached form a 5- to 7-membered heterocyclic ring which may optionally incorporate a carbon-carbon double bond or a further hetero atom linkage selected from O, S, NH, N(C1 -C4 alkyl) and N(C1 -C5 alkanoyl), and which may optionally be substituted with one to three substituents each independently selected from C1 -C4 alkyl and C1 -C4 alkoxy, and which may optionally be benzo-fused; X is CH2, CHCH3, C(OH)CH3, C=CH2 or O; m is 0 or 1; n is 0, 1, 2 or 3; and Het is 3- or 4-pyridyl or 1-imidazolyl; with the proviso that when Het is 1-imidazolyl then X is CH2 or CHCH3, are combined thromboxane A2 synthetase inhibitors and thromboxane A2 /endoperoxide antagonists of utility in the treatment of disease conditions in which thromboxane A2 is a causative agent.

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Reference£º
Copper catalysis in organic synthesis – NCBI,
Special Issue “Fundamentals and Applications of Copper-Based Catalysts”

 

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Process for producing 1,3,5-triaminobenzene

An aminobenzene is produced by reacting a chlorobenzene with ammonia in the presence of a copper type catalyst, namely by reacting ammonia with 3,5-diaminochlorobenzene to produce 1,3,5-triaminobenzene at a temperature of 150 to 250 C. at a molar ratio of ammonia of 2 to 10 to 3,5-diaminochlorobenzene in the presence of a copper compound catalyst.

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Reference£º
Copper catalysis in organic synthesis – NCBI,
Special Issue “Fundamentals and Applications of Copper-Based Catalysts”

 

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3-coxazolyl [phenyl, chromanyl or benzofuranyl]-2-hydroxypropionic acid derivatives and analogs as hypoglycemic agents

Certain 3-(phenyl, chroman-2-yl, benzofuran-5-yl, or benzoxazol-5-yl)-2-(hydroxy or mercapto)propionic acid derivatives and analogs are useful as hypoglycemic and hypocholesterolemic agents.

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Reference£º
Copper catalysis in organic synthesis – NCBI,
Special Issue “Fundamentals and Applications of Copper-Based Catalysts”

 

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Aromatic amino-alcohol derivatives having anti-diabetic and anti-obesity properties, their preparation and their therapeutic uses

Compounds of formula (I): STR1 (wherein: R0 is hydrogen, methyl or hydroxymethyl; R1 is substituted alkyl; R2 and R3 are each hydrogen, halogen, hydroxy, alkoxy, carboxy, alkoxycarbonyl, alkyl, nitro, haloalkyl, or substituted alkyl; X is oxygen or sulfur; and Ar optionally substituted phenyl or naphthyl); and pharmaceutically acceptable salts thereof have a variety of valuable pharmaceutical activities, including anti-diabetic and anti-obesity activities; in addition, they are capable of treating or preventing hyperlipemia and hyperglycemia and, by inhibiting the action of aldose reductase, they can also be effective in the treatment and prevention of complications of diabetes.

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Reference£º
Copper catalysis in organic synthesis – NCBI,
Special Issue “Fundamentals and Applications of Copper-Based Catalysts”

 

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Oxazolidine derivatives having anti-diabetic and anti-obesity properties, their preparation and their therapeutic uses

Compounds of formula (I): STR1 wherein: R is an alkyl group; X is oxygen or sulfur; Y is hydrogen atom or –A–COOH, in which A is an alkylene group; Ar is aryl or substituted aryl group; and pharmaceutically acceptable salts and esters thereof, have use in the treatment or prophylaxis of diabetes, obesity, hyperlipemia, hyperglycemia, complications of diabetes, obesity-related hypertension and osteoporosis.

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Reference£º
Copper catalysis in organic synthesis – NCBI,
Special Issue “Fundamentals and Applications of Copper-Based Catalysts”

 

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Theoretical studies on the electronic states of electron-doped copper oxides

The infinite layer copper oxides denoted as ACuO2, where A stands for the alkaline earth metal such as strontium or calcium, have attracted much attention in relation to high-temperature (Tc) superconductivity. Superconductivities of these species are achieved by several chemical doping such as hole-doping (h-doping) and electron-doping (e-doping). In this study, we have performed hybrid-density functional theory calculations, which are available in the strongly correlated systems such as transition metal complexes, in order to examine the electronic states after one e-doping for the linear chain clusters such as CuOCu and Cu3O2. The electronic states have been clarified from view points of energy, spin and charge density populations, natural orbital analysis and the difference of density. As the hole-doped electronic states have already been examined for the same clusters by the same methods in our previous work, we discuss the differences of the changes of electronic states between h-doping and e-doping.

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Reference£º
Copper catalysis in organic synthesis – NCBI,
Special Issue “Fundamentals and Applications of Copper-Based Catalysts”

 

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Benzothiophene compounds, intermediates, compositions, and methods

The present invention provides a method for inhibiting endometriosis comprising administering to a woman an effective amount of a compound of formula I STR1 wherein R1a is –H or –OR7a in which R7a is –H or a hydroxy protecting group; R2a is –H, halo, or –OR8a in which R8a is –H or a hydroxy protecting group; R3 is 1-piperidinyl, 1-pyrrolidino, methyl-1-pyrrolidinyl, dimethyl-1-pyrrolidino, 4-morpholino, dimethylamino, diethylamino, diisopropylamino, or 1-hexamethyleneimino; n is 2 or 3; and Z is –O– or –S–; or a pharmaceutically acceptable salt thereof.

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Reference£º
Copper catalysis in organic synthesis – NCBI,
Special Issue “Fundamentals and Applications of Copper-Based Catalysts”

 

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Thiazolidinedione derivatives, production and use thereof

A thiazolidinedione compound of the formula STR1 wherein X,Q are as defined in the specification. The compounds are used for treating diabetes.

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Copper catalysis in organic synthesis – NCBI,
Special Issue “Fundamentals and Applications of Copper-Based Catalysts”

 

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Substituted imidazo [1,2-a] pyridines

Certain novel substituted imidazo [1,2-a] pyridines with a substituted amino group at the 2- or 3-position are active anthelmintic agents. The novel compounds are prepared from the appropriate substituted 2-aminopyridine precursor. Compositions which utilize said novel imidazo [1,2-a] pyridines as the active ingredient thereof for the treatment of helminthiasis are also disclosed.

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Reference£º
Copper catalysis in organic synthesis – NCBI,
Special Issue “Fundamentals and Applications of Copper-Based Catalysts”