- 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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Paragraph 0049-0050
(2021/08/06)
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- Thiocyanation of aromatic and heteroaromatic compounds with 1-Chloro-1,2-benziodoxol-3-(1H)-one and (Trimethylsilyl)isothiocyanate
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Thiocyanation of aromatic compounds has been investigated using the combination of 1-chloro-1,2-benziodoxol-3-(1H)-one (1) and (trimethylsilyl)isothiocyanate (TMSNCS). The reaction with electron rich aromatic compounds proceeded smoothly to provide the th
- Ito, Yuta,Touyama, Akihiro,Uku, Minako,Egami, Hiromichi,Hamashima, Yoshitaka
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p. 1015 - 1018
(2019/09/12)
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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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Paragraph 0258; 0259; 0260; 0261; 0262; 0307-0311
(2019/06/17)
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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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- 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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- 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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- 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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- 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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- 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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- 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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