159 results about "Sulphonilamide" patented technology

The invention relates to N-hydroxysulfonamide derivatives that donate nitroxyl (HNO) under physiological conditions and are useful in treating and/or preventing the onset and/or development of diseases or conditions that are responsive to nitroxyl therapy, including heart failure and ischemia/reperfusion injury. Novel N-hydroxysulfonamide derivatives release NHO at a controlled rate under physiological conditions, and the rate of HNO release is modulated by varying the nature and location of functional groups on the N-hydroxysulfonamide derivatives.

The invention discloses a method for synthesizing perfluoroalkyl sulfimide alkali metal salt (M[Rf1SO2NSO2Rf2]) which is abbreviated to M[PFSI], wherein Rf1 and Rf2=CmF2m+1, m=1-8, M=Li, Na, K, Rb, and Cs. The method utilizes potassium (rubidium and cesium) salt of perfluoroalkyl sulfamide and perfluoroalkyl sulfonyl fluoride for reaction in the existence of potassium carbonate (rubidium and cesium), so that the potassium (rubidium and cesium) salt of the perfluoroalkyl sulfimide can be conveniently prepared with high yield which is 70-90%; the high-purity corresponding lithium (or sodium) salt (M[PFSI], M=Li and Na) can be obtained through double decomposition exchange reaction of the potassium (rubidium and cesium) salt and lithium perchlorate (or sodium) in aprotic polar solvent (such as acetonitrile, dimethyl carbonate, nitromethane and the like); and the hydrophobic functionalized ionic liquid composed of cations of sulfonium, ammonium or phosphorus with the [PFSI] through reaction of the prepared alkali metal salt and the sulfonium salt, ammonium salt or phosphorus salt of which the side chain contains functionalized functional groups.

The invention discloses sinomenine derivatives, and a preparation method and application thereof. The sinomenine derivatives are sinomenine derivative monomers or dimers formed by connecting the 4-position or 6-position carbon (C) of the frameworks of sinomenine and the conventional sinomenine derivatives with linker through X, wherein X is an ether bond, an ester bond, an amido bond, a sulfamide bond, or an amine bond and the like, and the linker is an aliphatic compound, an aromatic compound or polyethylene glycol and the like. The method for preparing the sinomenine derivatives is novel and unique, and simple and practicable; the prepared sinomenine derivatives have high purity and yield; when macrophages RAW264.7 in vitro are adopted to evaluate the NO inhibiting activity and anti-inflammatory action in rats, the sinomenine derivatives have high bioactivity, can be applied to preparing anti-inflammatory medicines for rheumatoid arthritis, rheumatic arthritis and the like, immunosuppressive agents and health products, have wide application range and good treatment effect, and have good social benefit.

There is provided a compound of Formula (I) wherein (I) R2 is selected from (i) an alkyloxyalkyl group (ii) a nitrile group, and wherein R2 is capable of forming a hydrogen bond (iii) alkylaryl group, wherein the aryl group is substituted by other than a C1-10 group (iv) alkenylaryl group wherein the aryl group is substituted (v) alkylheteroaryl group, wherein when heteroaryl group comprises only C and N in the ring, the aryl group is substituted by other than a methyl group (vi) alkenylheteroaryl group, (vii) ═N—O-alkyl or ═N—O—H group (viii) branched alkenyl (ix) alkyl-alcohol group (x) amide or alkylamide wherein (a) the alkyl of the alkylamide is —CH2— or —Ch2Ch2—, (b) the amide is di-substituted and/or (c) the amide is substituted with at least one of alkyl heterocycle group, alkenyl heterocycle group, alkylheteroaryl group, alkenylheteroaryl group, heteroaryl group, alkylamine group, alkyloxyalkyl group, alkylaryl group, straight or branched alkyl group, (xi) —CHO so that R1 together with R3 provide the enol tautomer (a); OR R2 together with R3 form (xii) a pyrazole wherein (a) R4 is ═N—O-alkyl or ═N—O—H group, (b) the pyrazole is substituted with one of alkyl-OH group, alkyl ester group, alkyloxyalkyl group, branched alkyl group, and an amide and/or (c) the 2 position is substituted with a group selected from —OH and —O-hydrocarbyl (xiii) a heteroaryl ring to provide a compound of the formula (b); (II) R2 is selected from groups capable of forming a hydrogen bond, a sulphamate group, a phosphonate group, a thiophosphonate group, a sulphonate group and a sulphonamide group; and (III) R3 is selected from —OH, ═O, or a C(═O)—mimetic.

The invention discloses a preparation method of azacyclo. The preparation method comprises the following steps of: (1) reacting diethylenetriamine or triethylene tetramine with methylsulfonyl chloride to generate methanesulfonamide; (2) during two-phase reaction, cyclizing compound catalytic cyclization on methanesulfonamide and a compound having the structure shown in a chemical formula (a) under the composite catalysis of benzyl triethylanmine compound and 15-crown-5 at 90 DEG C under a backflow condition; and (3) removing methylsulfonyl from methanesulfonamide azacyclo and performing methylation treatment, wherein X represents bromine, iodine or sulphonate. The preparation method has the advantages that raw materials are low in cost, atom economy is high, and operation is easy and safe. The preparation method is suitable for industrial production.

The invention provides a combination of polyethylene glycol and tamsulosin and a pharmaceutical compound comprising the combination which is as shown in a general formula (II). In the combination, a P and a P' are H or polyethylene glycol, and the P and the P' cannot be the H at the same time. The tamsulosin structurally contains a sulfamide group, the low-molecular-weight polyethylene glycol is introduced through an alkylation reaction, and therefore hydrophobicity of the tamsulosin is lowered, hydrophilism of the tamsulosin is increased, and the blood-brain barrier permeability of the tamsulosin is lowered. Therefore, the toxicity of the tamsulosin is lowered.

The present invention is based on the surprising finding that the linker employed in a bioconjugate, such as an anti-body-drug conjugate, is not therapeutically inert but has an effect on the therapeutic index of the bioconjugate. The present invention thus concerns a method for increasing the therapeutic index of a bioconjugate and the bioconjugates for use in treatment, in particular cancer. The bioconjugates according to the invention have a sulfamide linker comprising a group according to formula (1).

The invention provides dihydrothiazolone compounds containing sulfamide, represented by a formula (I), pharmaceutical compositions and use thereof. The compounds can be combined with proteins with bromodomain structural domains so as to adjust a downstream signal channel and exert a special function, and can be used for treating many diseases associated with bromodomain structural domains. The compounds can interfere combination of Brd4 with the bromodomain structural domain and an acetylized histone so as to down-regulate transcription of a cancer gene c-myc and associated target genes thereof, so that the compounds can become effective therapeutic drugs for treating tumors.

The invention discloses an application of benzene-sulfamide compounds in preparing an anti-HIV-1(human immunodeficiency virus-1) drug. A general formula of the benzene-sulfamide compounds is as shown in the specification, wherein X1-X4 are independently selected from halogen, H and -NO2, and have one -NO2 at the same time at most; X1-X4 are not halogen at the same time; R1 is selected from the substances as shown in the specification, wherein Y is C or N, n is an integer of 2-6, R3 is H or a statured chain hydrocarbon or a cyclic hydrocarbon with carbon number not exceeding 5, R4 is H or saturated chain hydrocarbons of C1-C4; R2 is selected from H, halogen or substance as shown in the specification; Y1 and Y2 are independently selected from H, halogen, and methyl. By applying the binding characteristic of Rev-RRE (response element), the inventor proves that the benzene-sulfamide compounds with the general formula can restrain Rev protein activity, causes expression quantity of luciferase in a screening system to reduce, and has a good antiviral effect. Moreover, powerful theoretical basis and practice basis are provided for further developing the antiviral drug, and therefore, the application has important development value and development significance.

The invention belongs to the technical field of organic synthesis, and concretely discloses a method for preparing pyrazole sulfamide type sodium, potassium and calcium metal complexes by an ultrasonic wave one-pot method and application. Pyrazolone ring amidogen is subjected to structure modification and solvent participation; a series of pyrazole sulfamide type sodium, potassium and calcium metal complexes are synthesized by the ultrasonic wave one-pot method. The metal coordination modes of sodium, potassium, calcium and the like are diversified; the coordination with nitrogen atoms and oxygen atoms on sulfamide is realized; the coordination with oxygen atoms on a solvent can also be realized; metal on the potassium complex can also be coordinated with halogen atoms on substitutional groups; the synthetized sulfamide type metal complexes based on a pyrazole framework have excellent biological activity; particularly, high activity is shown in the insect killing and antibiosis aspects, so that the synthetized sulfamide type metal complexes based on the pyrazole framework have great research and development and application values.