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ANTAGONISTS OF GONADOTROPIN RELEASING HORMONE

There are disclosed compounds of formula (I) STR1 and pharmaceutically acceptable salts thereof which are useful as antagonists of GnRH and as such may be useful for the treatment of a variety of sex-hormone related and other conditions in both men and women.

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Reference£º
Highly efficient and robust molecular ruthenium catalysts for water oxidation,
Catalysts | Special Issue : Ruthenium Catalysts – MDPI

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SUBSTITUTED ARYL 1,2,4-OXADIAZOLES DERIVATIVES AS SPHINGOSINE-1 PHOSPHATE RECEPTORS MODULATORS

The present invention relates to substituted aryl 1,2,4-oxadiazoles derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of sphingosine-1-phosphate receptors

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Reference£º
Highly efficient and robust molecular ruthenium catalysts for water oxidation,
Catalysts | Special Issue : Ruthenium Catalysts – MDPI

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Recent Advances in Cascade Reactions Initiated by Alcohol Oxidation

In this review, we attempt to answer the question: how can we construct complex functionalized molecules with significant added value from cheap and readily available alcohols in the simplest and most efficient manner? Accordingly, recent developments (mainly from the last five years) in the field of one-pot multiple transformations of alcohols are overviewed in terms of process simplification and optimization; sustainability; and atom, bond, step, and redox economy. Particular attention is paid to chemo- and stereoselective transformations with specific formation of particular bonds and configurations, leaving other parts of substrates unchanged.

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Reference£º
Highly efficient and robust molecular ruthenium catalysts for water oxidation,
Catalysts | Special Issue : Ruthenium Catalysts – MDPI

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HEXAHYDROPYRANO[3,4-d][1,3]THIAZIN-2-AMINE COMPOUNDS

The present invention provides compounds of Formula I, and the tautomers thereof, and the pharmaceutically acceptable salts of the compounds and tautomers, wherein the compounds have the structure wherein the variables R1, R2, R3, R4 and x are as defined in the specification. Corresponding pharmaceutical compositions, methods of treatment, methods of synthesis, and intermediates are also disclosed.

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Reference£º
Highly efficient and robust molecular ruthenium catalysts for water oxidation,
Catalysts | Special Issue : Ruthenium Catalysts – MDPI

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5-lipoxygenase inhibitors

Novel compounds having the ability to inhibit 5-lipoxygenase enzyme and having the following formula I: STR1 and the pharmaceutically acceptable salts thereof, wherein Ar1 is a heterocyclic moiety which is selected from imidazolyl, pyrrolyl, pyrazolyl, 1,2,3-triazolyl, 1,2,4-triazolyl, indolyl, indazolyl and benzimidazolyl, which is bonded to X1 through a ring nitrogen atom, and which may be optionally substituted with one or two substituents selected from halo, hydroxy, cyano, amino, and C1-4 alkyl; X1 is a direct bond or C1-4 alkylene; Ar2 is phenylene optionally substituted with halo, hydroxy, cyano, and amino X2 is –A–X– or –X–A– wherein A is a direct bond or C1-4 alkylene and X is oxy, thio, sulfinyl or sulfonyl; Ar3 is phenylene, pyridylene, thienylene, furylene, oxazolylene or thiazolylene optionally substituted with one or two substituents selected from halo, hydroxy, cyano, amino and C1-4 alkyl; R1 and R2 are each C1-4 alkyl, or together they form a group of formula –D1 –Z–D2 — which together with the carbon atom to which it is attached defines a ring having 3 to 8 atoms, wherein D1 and D2 are C1-4 alkylene and Z is a direct bond or oxy, thio, sulfinyl, sulfonyl, or vinylene, and D1 and D2 may be substituted by C1-3 alkyl; and Y is CONR3 R4, CN, C(R3)=N–OR4, COOR3, COR3 or CSNR3 R4, wherein R3 and R4 are each H or C1-4 alkyl. These compounds are useful in the treatment or alleviation of inflammatory diseases, allergy and cardiovascular diseases in mammals and as the active ingredient in pharmaceutical compositions for treating such conditions.

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Reference£º
Highly efficient and robust molecular ruthenium catalysts for water oxidation,
Catalysts | Special Issue : Ruthenium Catalysts – MDPI

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Process for the stereochemical inversion of (2S,3S)-2-amino-3-phenyl-1,3-propanediols into their (2R,3R) enantiomers

A four step process for transforming (2S,3S)-2-amino-3-phenyl-1,3–propanediols into their (2R,3R)-enantiomers is described. The final compounds are useful intermediates for the synthesis of antibiotics like Chloramphenicol, Thiamphenicol and Florfenicol. The starting products generally are discard products in the syn-thesis of said antibiotics.

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Reference£º
Highly efficient and robust molecular ruthenium catalysts for water oxidation,
Catalysts | Special Issue : Ruthenium Catalysts – MDPI

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4-aza-pregnane 5alpha-reductase isozyme 1 inhibitors

Compounds of formula (I), wherein: R1 is selected from the group consisting of hydrogen and methyl; R2 is selected from the group consisting of methyl and ethyl; R3 is selected from the group consisting of hydrogen and methyl; and the C1-C2 carbon-carbon bond may be a single or double bond. Such compounds are useful in the treatment of pathologic conditions that benefit from blockade of isozymes of 5alpha-reductase. STR1

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Reference£º
Highly efficient and robust molecular ruthenium catalysts for water oxidation,
Catalysts | Special Issue : Ruthenium Catalysts – MDPI

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Oxidation of primary alcohols to aldehydes with oxygen catalysed by tetra-n-propylammonium perruthenate

The liquid-phase oxidation of a series of saturated and unsaturated non-allylic alcohols to aldehydes with oxygen or air catalysed by tetra-n-propylammonium perruthenate (TPAP, represented as [(n-Pr)4N]RuO4) at 80-110 C is shown to proceed with selectivities of 72-91% at 55-80% alcohol conversion. The unsaturated alcohols, such as 9-decenol, 9-octadecenol and beta-citronellol, give the corresponding unsaturated aldehydes without competing double bond attack. The time course of oxidation indicates a complex reaction mechanism. The results on oxidation of a test alcohol, t-Bu(Ph)CHOH, suggest that one-electron processes do not play an important role in the TPAP-catalysed aerobic oxidation of alcohols.

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Reference£º
Highly efficient and robust molecular ruthenium catalysts for water oxidation,
Catalysts | Special Issue : Ruthenium Catalysts – MDPI

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Isolation, biological activities, and synthesis of the natural casuarines

This chapter describes the isolation, structure elucidation, glycosidase inhibitory activities, and the synthesis of the four naturally occurring casuarines. These are casuarine, casuarine-6-O-alpha-d-glucoside, 6-epi-casuarine (uniflorine A), and 3-epi-casuarine.

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Reference£º
Highly efficient and robust molecular ruthenium catalysts for water oxidation,
Catalysts | Special Issue : Ruthenium Catalysts – MDPI

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Inhibitors of protein isoprenyl transferases

Compounds having the formula or a pharmaceutically acceptable salt thereof wherein R1 is (a) hydrogen, (b) loweralkyl, (c) alkenyl, (d) alkoxy, (e) thioalkoxy, (f) halo, (g) haloalkyl, (h) aryl-L2?, and (i) heterocyclic-L2?; R2 is selected from(a) (b) ?C(O)NH?CH(R14)?C(O)OR15, (d) ?C(O)NH?CH(R14)?C(O)NHSO2R16,(e) ?C(O)NH?CH(R14)-tetrazolyl, (f) ?C(O)NH-heterocyclic, and(g) ?C(O)NH?CH(R14)?C(O)NR17R18; R3 is substituted or unsubstituted heterocyclic or aryl, substituted or unsubstituted cycloalkyl or cycloalkenyl, ?and ?P(W)RR3RR3?; R4 is hydrogen, lower alkyl, haloalkyl, halogen, aryl, arylakyl, heterocyclic, or (heterocyclic)alkyl; L1 is absent or is selected from (a) ?L4?N(R5)?L5?, (b) ?L4?O?L5?, (c) ?L4?S(O)n?L5?(d) ?L4?L6?C(W)?N(R5)?L5?, (e) ?L4?L6?S(O)m?N(R5)?L5?, (f) ?L4?N(R5)?C(W)?L7?L5?, (g) ?L4?N(R5)?S(O)p?L7?L5?, (h) optionally substituted alkylene, (i) optionally substituted alkenylene, (j) optionally substituted alkynylene (k) a covalent bond, (l) and (m) are inhibitors of protein isoprenyl transferases. Also disclosed are protein isoprenyl transferase inhibiting compositions and a method of inhibiting protein isoprenyl transferases.

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Reference£º
Highly efficient and robust molecular ruthenium catalysts for water oxidation,
Catalysts | Special Issue : Ruthenium Catalysts – MDPI