- Synthesis method of dithiobis-butyl phenol and analogue thereof
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The invention provides a synthesis method of dithiobis-butyl phenol and an analogue thereof. The synthesis method provided by the invention has the advantages of few steps, high yield and high purity of the obtained product. The dithiobis-butyl phenol and the analogue thereof synthesized by the invention can be used for preparing medicines for preventing and/or treating coronavirus pneumonia (containing COVID-19).
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- Probucol derivative, preparation method and application thereof
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The invention relates to the fields of compounds, and specifically relates to a probucol derivative, a preparation method and the application thereof. The probucol derivative has a structure shown asa general formula I. The probucol derivative provided by the invention can be used for prevention and curing of vascular diseases such as diabetes and cardiovascular and cerebrovascular diseases or complications thereof, can be used for reducing blood glucose, reducing blood fat, reducing cholesterol, reducing the weight, reducing triglyceride, resisting inflammation and oxidation and the like effectively, and has a wide application prospect.
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- Chemo- and product-selective electrooxidation of 3-(arylthiomethyl)- Δ3-cephems
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Electrolysis of 3-arylthiomethyl-Δ3-cephems possessing various substituents on the arylthio moiety undergo chemo selective and product-selective electrooxidation to give several different products. These include isomeric mixtures of the corresponding methoxylated cephems, a bis[(Δ3-cephem-3-yl)methyl]disulfide or a 3-dimethoxymethyl- Δ3-cephem. The selectivity of the oxidation is highly dependent on the nature of the substituents on the arylthio moiety which suggests that both steric and electronic effects play an important role in the electrooxidation of 3-arylthiomethyl-Δ3-cephems.
- Tanaka, Hideo,Tokumaru, Yoshihisa,Fukui, Ken-Ichi,Kuroboshi, Manabu,Torii, Sigeru,Jutand, Anny,Amatore, Christian
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experimental part
p. 3449 - 3459
(2010/02/28)
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- METHODS FOR PRODUCING 2,6-DI-TERT-BUTYL-4-MERCAPTOPHENOL AND 4,4'-ISOPROPYLIDENEDITHIOBIS[2,6-DI-TERT-BUTYLPHENOL]
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The present invention provides a method for producing 2,6-di-tert-butyl-4-mercaptophenol containing reducing bis(3,5-di-tert-butyl-4-hydroxyphenyl) polysulfide with zinc in a mixed solvent of toluene and n-butanol, and provides a method for producing 4,4'-isopropylidenedithiobis[2,6-di-tert-butylphenol] using the above-mentioned method.
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Page/Page column 4-5
(2008/06/13)
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- COMPOSITIONS AND METHODS FOR TREATING CARDIOVASCULAR DISORDERS
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The present invention relates to compounds and methods for the treatment of cardiovascular diseases and disorders. Compounds according to the present invention may comprise an optionally substituted phenyl ring linked to an aromatic or alkyl group by a spacer, wherein the spacer comprises two groups selected from selenium, sulfur, S(O) and S(O)2 and may further optionally comprise an alkylene, alkenylene, cycloalkylene or arylene moiety between the respective selenium, sulfur, S(O) and S(O)2 groups.
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Page/Page column 60
(2010/11/08)
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- Mechanism of the antioxidative effect of bis(4-hydroxy-3,5-di-tert-butylphenyl) sulfide and polysulfides in cumene oxidation
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Bis(4-hydroxy-3,5-di-tert-butylphenyl) sulfide and polysulfides were prepared, and their inhibiting power was studied in relation to the number of sulfur atoms.
- Farzaliev,Allakhverdiev,Sattar-zade,Rzaeva
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p. 2083 - 2086
(2007/10/03)
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- Antioxidant and cholesterol lowering properties of 2,6-di-t-butyl-4- [(dimethylphenylsilyl)methyloxy]phenol and derivatives: A new class of anti- atherogenic compounds
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Di-t-butylphenol derivatives were synthesized and evaluated as antioxidants and cholesterol lowering agents. When evaluated in cholesterol- fed rabbits, the compounds were found to exhibit both properties. Of special interest was the finding that several of the compounds elevated HDL cholesterol levels.
- Parker, Roger A.,Barnhart, Roger L.,Chen, Kim S.,Edwards, Michael L.,Matt Jr., James E.,Rhinehart, Barry L.,Robinson, Keith M.,Vaal, Mark J.,Yates, Mark T.
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p. 1559 - 1562
(2007/10/03)
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- Phenolic thioetheramides
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The present invention relates to phenolic thioetheramides of the formula STR1 wherein R1 and R2 are tert-alkyl or phenyl, Alk1 and Alk2 are alkylene; X is sulfur or oxygen, m is 0, 1, or 2; and R is STR2 wherein R3 and R4 are hydrogen or alkyl and Alk3 is alkylene.
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- 2-AMINOETHANESULFONIC ACID DERIVATIVES OF 3,5-DISUBSTITUTED-4-HYDROXY-PHENOLIC THIOETHERS
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The present invention relates to compounds of the Formula I:wherein R1 and R2 are the same or different and independently represent tert-alkyl, halogen, or phenyl; Alk 1 represents straight or branched chain alkylene of 2 to 10 carbon atoms which can optionally be substituted by hydroxy, provided that said hydroxy is not attached to a carbon which is adjacent to sulfur or oxygen, X represents sulfur or oxygen, and Alk 2 represents straight or branched chain alkylene of 1 to 4 carbon atoms; and the pharmaceutically acceptable salts thereof. These compounds are specific 5-lipoxygenase inhibitors and are useful as anti-inflammatory and anti-allergy agents and in the treatment of conditions mediated by 5-lipoxygenase
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- Method of stimulating superoxide generation
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The present invention is directed to a method of stimulating superoxide generation using phenolic thioethers which stimulate the generation of superoxide.
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- Process for preparing an intermediate useful in the syntheis of probucol
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A process for preparing 2,6-di-t-butyl-4-mercapto-phenol. This is accomplished by sulfonation of the phenol with a silylated sulfonating agent (e.g., trimethylsilyl-chlorosulfonate). The sulfonic acid is then reduced directly or is converted to the sulfonyl halide intermediate which is then reduced to yield the 2,6-di-t-butyl-4-mercapto-phenol.
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- Process for the preparation of 2,6-di-t-butyl-4-mercaptophenol
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In a process for preparing the 2,6-di-t-butyl-4-mercapto-phenol comprising (i) the sulfonation of 2,6-di-t-butyl-phenol, (ii) the optional preparation of an easily reducible derivative of the thus obtained 2,6-di-t-butyl-4-hydroxybenzenesulfonic acid, and (iii) the reduction of the 2,6-di-t-butyl-4-hydroxybenzenesulfonic acid or of an easily reducible derivative thereof, the improvement comprising carrying out step (i) with a silylated sulfonating agent.
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- 3,5-DITERTIARYBUTYL-4-HYDROXYPHENYL, 1,3,4-THIADIAZOLES AND OXADIAZOLES LINKED BY CARBON, OXYGEN, AND SULFUR RESIDUES
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The novel 3,5-ditertiarybutyl-4-hydroxyphenylthio-1,3,4-thiadiazoles and oxadiazoles and 3,5-ditertiarybutyl-4-hydroxyphenylmethanone-l,3,4-thiadiazoles and oxadiazoles and related compounds of the present invention are antiinflammatory agents having activity as inhibitors of 5-lipoxygenase, cyclooxygenase or both
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- Novel disubstituted 4-hydroxyphenylthio anilides
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The compounds of this invention are anilides represented by the formula: STR1 wherein: R1 and R2 are the same or different members of the group consisting of halo, phenyl, substituted phenyl and a STR2 group wherein n, m and p are independently an integer of from 1 to 8 provided that n+m+p is equal to or less than 10; X is thio, sulfinyl or sulfonyl; Alk is straight or branched chain lower alkylene; R3 is hydrogen or lower alkyl; and R4 is phenyl or substituted phenyl. The compounds of the present invention are useful in the treatment of inflammation, allergy and hypersensitivity reactions and other disorders of the immune system.
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- PHENOLIC THIOETHERS, SULFOXIDES, AND DISULFIDES AS INHIBITORS OF 5-LIPOXYGENASE
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The compounds of the present invention comprise substituted phenolic thioethers, sulfoxides, and disulfides that are specific inhibitors of 5-lipoxygenase and which, therefore, are useful in the treatment of local and systemic inflammation, allergy and hypersensitivity reactions and other disorders in which agents formed in the 5-lipoxygenase metablic pathway are involved
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- Acylaminoalkylpyridineamides as inhibitors of metastasis
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The present invention relates to a method of inhibiting tumor metastasis in an aminal by administering to an animal in need of such treatment an acrylaminoalkylpryridineamides represented by the formula STR1 wherein: R1 and R2 are the same or different members of the group consisting of halo, phenyl, substituted phenyl and a STR2 group wherein n, m and p are independently an integer of from 1 to 8 provided n+m+p is equal to or less than 10; x is thio or sulfinyl; Alk1 is straight or branched chain lower alkylene of 1 to 6 carbon atoms, R3 is hydrogen or lower alkyl, Alk2 is straight or branched chain alkylene of 1 to 4 carbon atoms; R4 is selected from the group consisting of hydrogen, halo, hydroxy, lower alkyl and lower alkoxy; or a pharmaceutically acceptable salt thereof, in an amount effective to inhibit tumor metastasis.
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- 5-LIPOXYGENASE INHIBITORS
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This invention encompasses compounds and methods for inhibiting lipoxygenase and includes a pharmaceutical composition comprising a pharmaceutical carrier and an effective lipoxygenase inhibiting amount of a compound of the formula: wherein R1 and R2 are the same or different members of the group consisting of tert-alkyl of 4 to 10 carbon atoms; and R3 is wherein R4 is hydrogen or lower alkyl; wherein R6 and R7 may be the same or different and are alkyl of 1 to 4 carbon atoms; or and the pharmaceutically acceptable salts thereof. The compounds and pharmaceutical formulations of the present invention are 5-lipoxygenase inhibitors and, therefore, are useful in the treatment of local and systemic inflammation, allergy and hypersensitivity reactions and other disorders in which agents formed in the 5-lipoxygenase metabolic pathway are involved.
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- Method of treating inflammation, allergy, asthma and proliferative skin disease using heterocyclic amides
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The compounds of this invention are heterocyclic amides represented by the formula: STR1 wherein: R1 R2 are the same or different members of the group consisting of halo, phenyl, substituted phenyl and a STR2 group wherein q, r and t are independently an integer of from 1 to 8 provided that q+r+t is equal to or less than 10; y is thio, sulfinyl or sulfonyl; Alk is straight or branched chain lower alkylene, and R3 is a heterocyclic amine represented by the formula: STR3 wherein R4 is selected from the group consisting of hydrogen, lower alkyl, phenyl, substituted phenyl, benzyl, substituted benzyl, carboxyl or carboxyloweralkyl; X is selected from the group consisting of N--R4, O and CH2 ; m is 2 or 3; n is 2 or 3 when X is O or N--R4, and n is 1 to 3 when x is CH2 ; p is 0 to 2; and the pharmaceutically acceptable salts thereof. The compounds are anti-inflammatory and anti-allergy agents.
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- Phenolic thioalkylamides as inhibitors of 5-lipoxygenase
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The compounds of the present invention comprise substituted phenolic thioalkylamides that are specific inhibitors of 5-lipoxygenase and which, therefore, are useful in the treatment of local and systemic inflammation, allergy and hypersensitivity reactions and other disorders in which agents formed in the 5-lipoxygenase metabolic pathway are involved.
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- Phenolic thioethers as inhibitors of 5-lipoxygenase
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The compounds of the present invention comprise substituted phenolic thioether derivatives that are specific inhibitors of 5-lipoxygenase and which, therefore, are useful in the treatment of local and systemic inflammation, allergy and hypersensitivity reactions and other disorders in which agents formed in the 5-lipoxygenase metabolic pathway are involved.
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- Phenolic thioethers as inhbitors of 5-lipoxygenase
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The compounds of the present invention comprise substituted phenolic thioether derivatives that are specific inhibitors of 5-lipoxygenase and which, therefore, are useful in the treatment of local and systemic inflammation, allergy and hypersensitivity reactions and other disorders in which agents formed in the 5-lipoxygenase metabolic pathway are involved.
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- Methods and compositions for inhibiting lipoxygenase
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This invention encompasses a pharmaceutical composition comprising a pharmaceutical carrier and an effective lipoxygenase inhibiting amount of a compound of the formula: STR1 wherein: R1 and R2 are same or different members of the group consisting of 1,1-dimethyl ethyl, halo, phenyl and substituted phenyl; Alk is straight or branched chain lower alkylene; R4 is hydrogen or lower alkyl; R3 is hydrogen or lower alkyl; or a cycloalkyl group of from 3 to 8 carbon atoms. The formulation of this invention are useful as anti-inflammatory and anti-allergy agents.
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- Novel phenolic thioethers as inhibitors of 5-lipoxygenase
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The compounds of the present invention comprise substituted phenolic thioethers represented by the formula: STR1 wherein: R1 and R2 are the same or different and independently represent tert-alkyl or phenyl; A represents methylene or methylene substituted by alkyl, dialkyl or hydroxy, provided that when A includes hydroxymethylene, the hydroxymethylene group is not adjacent to a heteroatom; B represents sulfur, sulfoxide, sulfone, oxygen, --NH-- or nitrogen substituted by alkyl, phenyl, benzyl, substituted phenyl or substituted benzyl; C represents methylene or methylene substituted by alkyl; R3 represents CO2 H, CO2 -alkyl or a tetrazole group; m is 0 or 1, n is 2, 3 or 4 and p is 1, 2 or 3; and the pharmaceutically acceptable salts thereof. The compounds of the present invention are specific inhibitors of 5-lipoxygenase and, therefore, are useful in the treatment of local and systemic inflammation, allergy and hypersensitivity reactions and other disorders in which agents formed in the 5-lipoxygenase metabolic pathway are involved.
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- S-(HYDROXYMETHYL) 4-HYDROXYPHENYL SULFIDES: SYNTHESIS AND SELECTED CHEMISTRY OF SOME STABLE HEMIMERCAPTALS
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The base-catalyzed reaction of 3,5-di-tert-butyl-4-hydroxybenzenethiol (1a), 3-tert-butyl-4-hydroxy-5-methylbenzenethiol (1b), and 4-hydroxybenzenethiol (1c) with formaldehyde gave the corresponding hemimercaptal derivatives 2a-c, respectively.The stable hemimercaptals 2a-c were characterized by IR, 1H NMR, 13C NMR, MS and elemental analysis.The ester of 2a with 3-(3,5-di-tert-butyl-4-hydroxyphenyl)propanoic acid (3a) was prepared using triphenylphosphine and diethyl azodicarboxylate (Mitsunobu conditions).
- Pastor, Stephen D.,Odorisio, Paul A.,Ravichandran, Ramanathan
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- Phenolic thioethers as inhibitors of 5-lipoxygenase
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The compounds of the present invention comprise substituted phenolic thioethers represented by the formula: STR1 wherein: R1 and R2 are the same or different and independently represent tert-alkyl or phenyl; A represents methylene or methylene substituted by alkyl, dialkyl or hydroxy, provided that when A includes hydroxymethylene, the hydroxymethylene group is not adjacent to a heteroatom; B represents sulfur, sulfoxide, sulfone, oxygen, --NH-- or nitrogen substituted by alkyl, phenyl, benzyl, substituted phenyl or substituted benzyl; C represents methylene or methylene substituted by alkyl; R3 represents CO2 H, CO2 -alkyl or a tetrazole group; m is 0 or 1, n is 2, 3 or 4 and p is 1, 2 or 3; amd the pharmaceutically acceptable salts thereof. The compounds of the present invention are specific inhibitors of 5-lipoxygenase and, therefore, are useful in the treatment of local and systemic inflammation, allergy and hypersensitivity reactions and other disorders in which agents formed in the 5-lipoxygenase metabolic pathway are involved.
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- Acylaminoalkylpyridines ad use in treatment of inflammation and allergy reactions
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The compounds of this invention are acylaminoalkylpyridines representd by the formula STR1 wherein: R1 and R2 are the same or different members of the group consisting of halo, phenyl, substituted phenyl and a STR2 group wherein n, m and p are independently an integer of from 1 to 8 provided n+m+p is equal to or less than 10; X is thio, sulfinyl or sulfonyl; Alk1 is straight or branched chain lower alkylene of 1 to 6 carbon atoms, R3 is lower alkyl, Alk2 is straight or branched chain alkylene of 1 to 4 carbon atoms; R4 is selected from the group consisting of hydrogen, halo, hydroxy, lower alkyl and lower alkoxy; and the pharmaceutically acceptable salts thereof. The compounds of the present invention are useful in the treatment of inflammation, allergy and hypersensitivity reactions and other disorders of the immune system.
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- Cardiotonic and antithrombotic sulfur-containing derivatives of carbostyril
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Compounds of the formula STR1 wherein W is vinylene, methyl-vinylene, methylene or ethylene; m is 0, 1 or 2; D is straight or branched alkylene of 2 to 6 carbon atoms, straight or branched hydroxy-alkylene of 3 to 6 carbon atoms, or xylylene; R1 is hydrogen or alkyl of 1 to 3 carbon atoms; R2 is cycloalkyl of 3 to 6 carbon atoms, aryl of 6 to 10 carbon atoms, aralkyl of 7 to 11 carbon atoms, heteroaryl, heteroarlkyl, 1,2,4-triazolyl, triphenylmethyl, 4,5-bis-(p-chlorophenyl)-oxazol-2-yl, N-methyl-cyclohexylamino-carbonylmethyl,-amino-iminomethyl or, when m is 1 or D is hydroxyalkylene or xylylene, also alkyl of 1 to 6 carbon atoms; and R3 and R4 are each hydrogen, halogen, alkyl of 1 to 4 carbon atoms, amino, acetylamino or nitro. The compounds of the invention are useful as cardiotonics and as antithrombotics.
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