- The promoted synthesis of minoxidil by magnetic nanoparticles of cobalt ferrite (CoFe2O4) as a heterogeneous reusable catalyst
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Minoxidil (2,4-diamino-6-piperidinopyrimidine 3-oxide) was primarily recognized as a drug for reducing vascular resistance to blood flow. It was later introduced as a more important medicine for topical stimulation of hair growth and baldness reverting as well as treatment of androgenic alopecia through increasing prostaglandin endoperoxide synthesis. In this study, magnetic nanoparticles (MNPs) of spinel ferrites (MFe 2 O 4, M = Co, Ni, Fe, Cu, and Zn) via solid-state grinding procedure were prepared and then characterized using X-ray diffraction, scanning electron microscopy, transmission electron microscopy, vibrating sample magnetometer, and Fourier transform infrared techniques. The prepared nanoferrites were utilized as efficient and green heterogeneous catalysts for N -oxidation of 2,6-diamino-4-chloro-pyrimidine with H 2 O 2 in refluxing ethanol giving 2,6-diamino-4-chloro-pyrimidine N -oxide as a starting material for the synthesis of 2,4-diamino-6-piperidinopyrimidine 3-oxide (minoxidil). Among the examined nanoferrites, CoFe 2 O 4 MNPs exhibited prominent catalytic activity giving the product in 95% yield within 60 min. Moreover, the reusability of nano-CoFe 2 O 4 was examined for 6 consecutive cycles without significant loss of catalytic activity and magnetic property.
- Eisavi, Ronak,Ahmadi, Fatemeh,Zeynizadeh, Behzad,Kouhkan, Mehri
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p. 1425 - 1435
(2019/11/02)
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- METHOD OF ENHANCING HAIR GROWTH
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Methods and compositions for stimulating the growth of hair are disclosed wherein said compositions include bimatoprost and minoxidil in a vehicle for topical application to the skin of a mammal, e.g. a human, whereby the combination of bimatoprost and minoxidil produces a faster onset of hair growth in humans or other mammals and wherein said composition brings about a synergestic result of faster onset of hair growth as compared to compositions comprising bimatoprost and minoxidil, alone.
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- Nanoparticles comprising half esters of poly (methyl vinyl ether-co-maleic anhydride) and uses thereof
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The present invention relates to nanoparticles for encapsulating compounds, the preparation and uses thereof, said nanoparticles being based on half (C1-C4) alkyl esters of poly (methyl vinyl ether-co-maleic anhydride) (PVM/MA) copolymers. Said nanoparticles can encapsulate or incorporate a product of interest. For use in the agricultural, cosmetic, food or pharmaceutical fields.
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- 3-deoxyglucosone and skin
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The invention relates to a method of removing 3-deoxyglucosone and other alpha-dicarbonyl sugars from skin. The invention further relates to methods of inhibiting production and function of 3-deoxyglucosone and other alpha-dicarbonyl sugars in skin. The invention also relates to methods of treating 3-deoxyglucosone and other alpha-dicarbonyl sugars associated diseases and disorders of skin.
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- Scalp life conditioner
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The present invention is an improved scalp conditioner for conditions related to flaky and inflamed scalp that are commonly associated with dandruff, seborrhea, psoriasis and burns from the use of alkaline based products. The method involves administering the product to the scalp of the head and gently massaging the scalp. It can be administered several times per week.
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- Topical delivery systems for active agents
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This invention relates to a method for enhancing the transmembrane penetration of benefit agents using a certain non-ionic lipid/surfactant-containing formulation as an enhancing agent, and the compositions used therein. Various active agents, such as anti-dandruff agents, hair growth agents, hair inhibitor agents, anti-acne agents, anti-aging agents, depilatory agents, and depigmentation agents, may be effectively delivered into the skin, hair follicles and sebaceous glands using the compositions of the present invention.
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- Relative Reactivity in Piperidino-Dechlorination of 2,4-Diamino-6-chloropyrimidine, 2,4-Diamino-6-chloropyrimidine N(3)-Oxide, and Their Acetylamino Analogues
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The second-order rate constants kA for the piperidino-dechlorination of 2,4-diamino-6-chloropyrimidine (1a), 2,4-bis(acetylamino)-6-chloropyrimidine (1b), 2,4-diamino-6-chloropyrimidine N(3)-oxide (2a), and 2,4-bis(acetylamino)-6-chloropyrimidine N(3)-oxide (2b) have been determined from the corresponding pseudo-first-order rate constants, kψ, measured in DMSO at 21.0 deg C by the UV spectrophotometric procedure.The second-order rate coefficients of the less reactive substrates 1a and 2a at 21 deg C have been obtained as extrapolated values from Arrhenius plots of kA values, calculated through the psudo-first-order-type relationship, kψ = kA(where is the amine concentration),from the kψ measured at higher temperatures (kA(1a) = 1.36E-5 and kA(2a) = 3.44E-5 L mol-1 min -1).The reactivities of the acyl derivatives 1b and 2b are remarkably higher than that of the parent compounds 1a and 2a.The pseudo-first-order-rate constants of the more reactive substrates 1b and 2b, measured as a function of piperidine concentration, increase linearly for 1b, with a decreasing curvilinear slope only in the higher concentration region of base; in contrast, the reactivity of 2b remains almost constant and lower than that of 1b for most of the employed base concentrations.This behavior is due to the acidic character of compound 2b, which is almost totally transformed by excess piperidine into an anionic form, much less reactive than the protonated one toward the nucleophilic attack, even at relatively low base concentrations.Compound 1b is much less acidic than 2b and shows deviations from the second-order-type linear behavior only for the higher base concentrations.The equilibrium constant for the acid-base reaction of 2b with piperidine has been obtained spectrophotometrically (K= 0.007 +/- 0.001), and the second-order rate coefficient kA has been calculated from the constant apparent reactivity kψ by means of the formula kA = kψ/K (where is the piperidinium ion concentration) (kA(2b) = 2.7 L mol-1 min-1).That of 1b is given by the slope of the experimental curve kψ vs in the proximity of the origin (kA(1b) = 0.15 L mol-1 min-1).The results indicate that both the acetylation of the exocyclic -NH2 groups and the oxidation of the cyclic N(3)-atom increase the reactivity of the parent compounds toward piperidinolysis, but that the first modification is much more effective than the second one.The dependence of kψ of 1b and 2b on the amine concentration does not give any evidence for base catalysis, as expected in the model of the intermediate complex mechanism when the leaving group is fast to separate (as the -Cl group is) and/or the complex formation is rate-limiting.
- Maltese, M.
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p. 2436 - 2442
(2007/10/02)
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- Minoxidil gel
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The present invention provides a novel pharmaceutically acceptable gel containing minoxidil for topical application.
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- Cosmetic composition comprising an ester of pyroglutamic acid
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A preserved composition suitable for topical application to mammalian skin or hair for inducing, maintaining or increasing hair growth comprises: (i) a special ester of pyroglutamic acid; and (ii) a cosmetically acceptable vehicle for the ester.
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- Amino-substituted pyrimidines, derivatives and methods of use therefor
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The present invention relates to compositions and methods for inhibiting nonenzymatic cross-linking (protein aging). Accordingly, a composition is disclosed which comprises an agent capable of inhibiting the formation of advanced glycosylation end products of target proteins by reacting with the carbonyl moiety of the early glycosylation product of such target proteins formed by their initial glycosylation. The method comprises contacting the target protein with the composition. Both industrial and therapeutic applications for the invention are envisioned, as food spoilage and animal protein aging can be treated.
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- Hair growth composition containing citric acid esters
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Triesters of citric acid are used for inducing, maintaining or increasing hair growth. Compositions for topical application to mammalian hair or scalp comprise an effective amount of from 1% to 99% by weight of an ester of citric acid having the structure (1): where, R1, R2 and R3 each independently represent a branched or unbranched alkyl, alkenyl, aryl, alkylaryl or arylalkyl group, each said group having from 1 to 18 carbon atoms, R4 represents -H, or a branched or unbranched saturated or unsaturated acyl, alkyl, aryl, alkylaryl or aylalkyl group having from 1 to 18 carbon atoms, in the presence of a cosmetically acceptable vehicle for the citric acid ester and in the absence of solid absorbent for the ester;, said effective amount of said ester being sufficient to increase hair growth in the rat, when said composition is applied topically thereto over a period of no more than three months, by at least 10% more than that obtainable using a control composition from which the said ester has been omitted, in accordance with the Rat Hair Growth Test.
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- Process for the preparation of 6-piperidino-2,4-diamino pyrimidine-3-oxide
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In a first stage of a process for the preparation of 6-piperidino-2,4-diaminopyrimidine-3-oxide at least one of the two amino groups of a compound having formula (1): STR1 where x represents a halogen atom or OH group, is protected by an addition reaction with an isocyanate having formula: In this formula R represents an alkyl group, or one of the amino groups. The resulting urea derivative is then oxidized to produce the corresponding N-oxide which is then reacted with piperidine. The protective group(s) are then eliminated by reaction with an organic or inorganic base.
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- Method for the preparation of a therapeutically active compound
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A method for the preparation of 2,4-diamino-3-oxy-6-piperidyl-pyrimidine or minoxidil wherein a compound of the formula STR1 wherein R is a C1-4 alkyl or a phenyl group optionally having up to three C1-4 alkyl substituents, is oxidized to a compound of the formula STR2 which according to known methods is reacted with piperidine to minoxidil. In the inventive method magnesium monoperoxyphthalate, which has the formula STR3 is used as the oxidizing agent.
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- Slow-release topical formulations
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Salts of 2,4-diamino-6-piperidino-pyrimidine-3-oxi-de (minoxidil) with hydrosoluble polyanions such as poly-styrenesulfonates, polyacrylates, polyphosphates, polyvi-nylsulfonates, sulfates or phosphates and polydextransul-fates are described. The salts according to the invention, prepared by precipitation from aqueous solutions having pH generally lower than 4.5, show chemico-physical characteristics supporting an advantageous use as slow-release active principles, in topical pharmaceutical compositions endowed with higth coating potency, of occlusive kind, to be used in the prevention and treatment of alopecia and of hair loss.
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- Pharmaceutical composition and process of treatment
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A process for alleviating proliferative skin diseases such as psoriasis, atopic dermatitis, etc. comprising administering to humans, or domesticated animals, topically and/or systemically a composition comprising a pharmaceutical carrier and at least one active compound selected from the groups, substituted alkyl zanthines, tricyclic antidepressants, organic nitrates, antihypertensives, anti-asthma agents and central nervous system depressants and combinations of certain compounds from specifically named groups of compounds.
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