310 results about "Sulfamide" patented technology

The present invention is directed to novel sulfamide and sulfamate derivatives, pharmaceutical compositions containing them and their use in the treatment of epilepsy and related disorders.

A class of acyl sulfamides comprises compounds that are potent ligands for PPAR gamma and generally have antagonist or partial agonist activity. The compounds may be useful in the treatment, control or prevention of obesity, non-insulin dependent diabetes mellitus (NIDDM), hyperglycemia, dyslipidemia, hyperlipidemia, hypercholesterolemia, hypertriglyceridemia, atherosclerosis, vascular restenosis, inflammation, and other PPAR gamma mediated diseases, disorders and conditions.

The present invention is directed to novel sulfamide and sulfamate derivatives, pharmaceutical compositions containing them and their use in the treatment of epilepsy and related disorders.

The invention relates to a novel linker for use in bioconjugates such as antibody-drug-conjugates. The linker according to the invention is represented by formula: (I) wherein: —BM is a branching moiety; —E is a capping group; —SG is a sulfamide group; —b, c, d, e, g, i, k, l are independently 0 or 1; —f is an integer in the range of 1 to 10; —Sp1, Sp2, Sp3, Sp4, Sp5 and Sp6 are a spacer moieties; —Z and Z2 are connecting groups. The linker according to the invention is useful in the preparation of linker-conjugates and bioconjugates, and can be used for (a) improving conjugation efficiency in the preparation of the bioconjugate, (b) reducing aggregation during the preparation of the bioconjugate and / or of the bioconjugate, (c) increasing stability of the bioconjugate, and / or (d) increasing therapeutic index of the bioconjugate.

The invention provides a sulfur / nitrogen double-doped carbon quantum dot with high fluorescence quantum yield and a preparation method and ion detection application of the sulfur / nitrogen double-doped carbon quantum dot. The carbon source of the carbon quantum dot is provided from sodium citrate, and the sulfur source and the nitrogen source of the carbon quantum dot are both provided from sulfamide. The reparation method comprises the following steps: dissolving the raw materials in a hydrothermal reaction kettle for reaction, after the synthesized product is naturally cooled, separating so as to obtain a solution, and drying the solution, thereby obtaining the sulfur / nitrogen double-doped carbon quantum dot with high fluorescence quantum yield. By adopting the method, only one step of reaction is needed, a small amount of middle products and byproducts can be generated, a very small amount of raw materials is needed, the reaction speed is fast, and the method is both economic and environment-friendly. In addition, the sulfur / nitrogen double-doped carbon quantum dot has the characteristics of high fluorescence quantum yield, can be successfully applied to detection on Hg<2+>, and has wide application prospect in biological detection, sewage treatment and the like.

The invention discloses a preparation method for lithium bis(fluorosulfonyl)imide. The preparation method comprises the following steps: 1) preparing fluorine sulfamide lithium; 2) preparing sulfuryl fluoride, and pumping the sulfuryl fluoride into the fluorine sulfamide lithium solution, and adding an acid-binding agent to prepare bifluorine sulfimide ammonium salt; 3) dissolving the bifluorine sulfimide ammonium salt in water solution, to obtain bifluorine sulfimide water solution through the acid resin exchange; 4) adding lithium carbonate, regulating the PH value to be neutral, filtering and removing undissolved substances, depressurizing and removing the most of the water, and adding a weak-polarity organic solvent to separate out a coarse product of the lithium bis(fluorosulfonyl)imide, further depressurizing and drying; and 5) adding a polarity solvent to the coarse product of the lithium bis(fluorosulfonyl)imide, stirring and dissolving, filtering and removing the undissolved substances, depressurizing and removing a strong-polarity solvent, and adding the weak-polarity organic solvent to perform the recrystallization, and depressurizing and drying to obtain a product after filtering. The preparation method is simple, the reaction time is short, the yield is high, and metal ion and negative ion impurities can be effectively controlled, so that the product with the high purity can be obtained.

The present invention is directed to novel benzo-fused heteroaryl sulfamide derivatives, pharmaceutical compositions containing them and their use in the treatment of epilepsy and related disorders. The present invention is further directed to a crystalline form of N-(benzo[b]thien-3-ylmethyl)-sulfamide and a process for its preparation.

The invention discloses a method for preparing bis(sulfonyl fluoride) imine and (perfluoroalkyl sulfonyl fluorine sulfonyl) imine alkali metal salt. According to the method, sulfamide is utilized to take reaction with thionyl chloride and chlorosulfonic acid for preparing bis(sulfonyl fluoride) imine or (perfluoroalkyl sulfonyl fluorine sulfonyl) imine, then, the bis(sulfonyl fluoride) imine or (perfluoroalkyl sulfonyl fluorine sulfonyl) imine takes reaction with antimony trifluoride and potassium (rubidium or caesium and the like) carbonate, and corresponding high-purity bis(sulfonyl fluoride) imine potassium (rubidium or caesium) salt or (perfluoroalkyl sulfonyl fluorine sulfonyl) imine potassium (rubidium or caesium) salt can be obtained; and the double decomposition exchange reaction of the potassium (rubidium or caesium) salt and lithium (or sodium) perchlorate or lithium (or sodium) tetrafluoroborate and the like in aprotic polar solvents is utilized to obtain corresponding high-purity lithium (or sodium) salt. The method provided by the invention has the characteristics that the operation step is simple, the products can be easily separated and purified, the purity and the yield are high, the environment pollution is avoided, the method is suitable for industrial mass production, and the like.

The present invention relates to oxo fluoroalkyl sulfonamide compound and its preparation process and use as household and farm chemical pesticide. Structurally, the compound is perfluoro sulfonamide compound with increased ether bond structure. It has simple synthesis process. The pesticidal activity test shows that the oxo fluoroalkyl sulfonamide compound has increased roach killing activity and plant hopper preventing and controlling bioactivity, so that it may be used in preparing household and farm chemical pesticide.

Sulfamide compounds having formula (I) are described as well as their use in the treatment of diseases dependent on the signaling pathways associated with .beta.-adrenergic receptors, such as obesity, diabetes, hypertension, gastrointestinal hypo- or hyper-motility and cardiovascular diseases. 1

The present invention relates to a compound comprising an alpha-end and an omega-end, the compound comprising on the alpha-end a reactive group Q1 capable of reacting with a functional group F1 present on a biomolecule and on the omega-end a target molecule, the compound further comprising a group according to formula (1) or a salt thereof:Said compound may also be referred to as a linker-conjugate. The invention also relates to a process for the preparation of a bioconjugate, the process comprising the step of reacting a reactive group Q1 of a linker-conjugate according to the invention with a functional group F1 of a biomolecule. The invention further relates to a bioconjugate obtainable by the process according to the invention.

The present invention is a method for the treatment of alcohol abuse and / or addiction comprising administering to a subject in need thereof a therapeutically effective amount of one or more novel benzo-fused heterocycle sulfamide derivatives of formula (I) and / or formula (II) as herein defined.

The invention provides a method for preparing baricitinib. The method comprises the following steps: by taking 4-pyrazol boric acid pinacol ester (10) as an initial raw material, performing Michael addition reaction on the initial raw material and 3-(icyanomethylene) azacyclo-cyclobutane-1-tert-butyl formate (11) so as to prepare an intermediate 12, and performing catalytic coupling reaction on 12 and 13, thereby preparing an intermediate 14; removing two-molecule tert-butyl formate of the intermediate 14, thereby preparing an intermediate 15; performing sulfamide reaction on the intermediate 15 and ethanesulfonyl chloride in an organic solvent, thereby obtaining a final product baricitinib (1). The method for preparing baricitinib has the advantages that the raw materials are easy to obtain, the process is simple, the operation is convenient, the reaction yield is high when being compared with that of document records, the atom utilization rate is high, industrial production can be easily achieved, and the like. The reaction general formula is as shown in the specification.

N-(3,5-bis-disubstituted aminomethyl-4-hydroxy)benzyl aromatic sulfonamides and N-(3,5-bis-disubstituted aminomethyl-4-hydroxy)phenyl aromatic sulfonamides compounds in accordance with the animal test, are active in the prevention and the treatment of cardiac arrhythmia. These compounds are prepared as corresponding diamines by the condensation of optionally substituted aromatic sulfochlorides with p-hydroxybenzylamine, p-aminophenol, or the like, which followed by the Mannich reaction of the resulted corresponding aromatic sulfamides with formaldehyde and secondary amines; or directly obtained by the reaction of the aromatic sulfamides with 4-amino-2,6-bis-disubstituted aminomethylphenol. Subsequently, the diamines are reacted with various acids to provide their salts.

The present invention is a method for treating, preventing, reversing, arresting or inhibiting the occurrence, development and maturation of seizures or seizure-related disorders. More specifically, the present invention is directed to methods for the use of benzo-fused heterocycle sulfamide derivatives of formula (I) and formula (II) as described herein to therapeutically or prophylactically treat, prevent, reverse, arrest or inhibit epileptogenesis and epilepsy.

The invention discloses a fluorine-carbon gemini surfactant for oil extraction and a preparation method thereof. The preparation method of the surfactant is as follows: 1) perfluorooctsulfunyl fluoride is dissolved in ethyl acetate, is firstly mixed with polyethylene polyamines and then reacts with potassium hydroxide after being heated to obtain diperfluoro octyl sulfamide; 2) diperfluoro octyl sulfamide is mixed with 2-chlorethanol in an organic solvent and reacts with potassium hydroxide to obtain N-N-alcohol diperfluoro octyl sulfamide; 3) N-N-alcohol diperfluoro octyl sulfamide is mixed with hydrogen peroxide and reacts with potassium hydroxide to obtain the target product. The fluorine-carbon gemini surfactant for oil extraction provided by the invention has comparatively low using concentration, can obviously reduce the surface tension of aqueous phase system, is excellent in temperature and salt resistance, can be used as a surfactant component in polymer-surfactant binary compound flooding and alkali-polymer-surfactant ternary compound flooding systems and can also be directly applied in surfactant flooding.

The present invention is a methods for neuroprotection, for treating an acute neurodegenerative disorder, for treating a chronic neurodegenerative disorder and / or for preventing neuron death or damage following brain, head and / or spinal cord trauma or injury comprising administering to a subject in need thereof a therapeutically effective amount of one or more novel benzo-fused heterocycle sulfamide derivatives of formula (I) and formula (II) as herein defined.

The invention belongs to the field of chemistry, and relates to a method for testing the nitrite and nitrate in pickled vegetables. The method for rapidly testing the nitrite and nitrate in pickled vegetables comprises the following steps that: (1) the nitrite and the nitrate in pickled vegetable are extracted by ultrasonic waves; (2) a calibration curve is drawn by using nitrosonitrogen (NO2-) standard solution; and a calibration curve is drawn by using nitronitrogen (NO3-) standard solution; (3) by diazotizing sulfamide, the nitrite in the pickled vegetable is coupled with hydrochloric acid N-(1-naphthyl)ethylenediamine, so that rosy azo dye is produced, and the content of the nitrite is determined at 540nm; (4) the nitrate in the pickled vegetable is reduced to nitrite by a cadmium column, the nitrite is determined, the determined nitrite in the same sample is subtracted, and the nitrate content is worked out.

The present invention is a method for the glucose related disorders and lipid related disorders comprising administering to a subject in need thereof a therapeutically effective amount of one or more novel benzo-fused heterocycle sulfamide derivatives of formula (I) or formula (II) as herein defined. The present invention is further directed to methods of treatment comprising co-therapy with an anti-diabetic agent, and anti-lipid agent and / or an anti-obesity agent.

It is intended to provide a compound represented by the following general formula (1) or a pharmaceutically acceptable salt thereof. Because of having a sufficiently high antitumor activity, this compound or its salt is useful as a remedy for cell proliferative diseases, in particular, cancer. It is also intended to provide a medicinal composition which contains the above-described compound or its salt as the active ingredient. [Chemical formula 1] (1) wherein X is selected from heteroaryl, etc.; Y<1> and Y<2> are selected from -N=, etc.; Y<3> and Y<4> are selected from -CH=, etc.; A is selected from sulfamide, etc.; R<1> is selected from hydrogen, etc.; and R<2> is selected from C1-6 alkyl, etc.

Novel indansulfamide derivatives or a pharmaceutically acceptable salt thereof such as N-[(1S)-2,2,5,7-tetrafluoro-2,3-dihydro-1H-inden-1-yl]sulfamide, N-[(1S)-2,2,4,7-tetrafluoro-2,3-dihydro-1H-inden-1-yl]sulfamide, (+)-N-(2,2,4,6,7-pentafluoro-2,3-dihydro-1H-inden-1-yl)sulfamide, have an action of improving Seizure Severity Index (Score) in mice kindling model. Thus the compounds or the salt thereof are expected as a drug for treating epilepsy.

The invention relates to a process for preparing a fluoro compound of formula:R2—(SO2)—NX—(SO2)—F   (III)comprising:(a) a first step for obtaining the chloro compound of formula:R1—(SO2)—NX—(SO2)—Cl;   (II)this first step comprising the reaction of the sulfamide of formula:R0—(SO2)—NH2   (I)with a sulfureous acid and a chlorinating agent; and(b) a second step for obtaining the fluoro compound of formula (III), this second step comprising the reaction of the chloro compound of formula (II) with anhydrous hydrofluoric acid in at least one organic solvent;in which:X represents either a hydrogen atom or a monovalent cation M;R1 represents an electron-withdrawing group having a positive Hammett parameter σp;if R1 represents Cl, then R0 represents OH; otherwise, R0 is identical to R1; andif R1 represents Cl, then R2 represents F; otherwise, R2 is identical to R1.

The invention discloses a tanshinone IIA derivative. A connecting arm, phosphocreatine and an analogue of the phosphocreatine form a conjugate of which the structure is as shown in formula (I) in the specification, wherein n is equal to 1-3, m is equal to 0-3, R1 and R2 respectively independently represent hydrogen atoms, C1-C5 alkyl, cycloalkyl, vinyl and alkynyl, the R1 and the R2 also can form ternary to hexatomic rings, and M represents metal ions, like sodium ions. The compound can be used for improving the water solubility of the whole molecule through sodium phosphate in the phosphocreatine on the premise of maintaining the activity of the tanshinone IIA; moreover, a phosphocreatine fragment in the molecule can play a dual protection effect on myocardial muscles.

The present invention is directed to novel sulfamide derivatives, pharmaceutical compositions comprising said compounds and methods for the treatment of epilepsy and related disorders comprising administering to a subject in need thereof, said compounds, either alone or as co-therapy with one or more anticonvulsant and / or anti-epileptic agents.

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 a chemical oxygen demand (COD) degradation agent for removing sulfamide from industrial wastewater in the field of environment sewage treatment. The degradation agent is formed by compounding the following components in percentage by mass: 70 to 85 percent of inorganic strong oxidant, 1 to 5 percent of catalyst and 10 to 29 percent of genetic engineering bacteria enzyme, wherein the inorganic strong oxidant is one or two of sodium chlorate, potassium ferrite, ammonium persulfate and sodium bismuthate; the catalyst is one of nickel oxide, copper oxide, titanium oxide and lead oxide; the genetic engineering bacteria enzyme is one or two of cyclic amide hydrolase, lignocellulose hydrolase, protein hydrolase, organic phosphorus hydrolase and amylase; and the wastewater is added with 1 to 5 percent of degradation agent and continuously stirred, so that the concentration of the sulfamide in the wastewater is reduced to below 0.5mg / L from 1,000mg / L, and the removal rate is more than 99.9 percent. The degradation agent is easy to use and cannot produce secondary pollution; raw materials are readily available; and precipitates are not produced.

The invention discloses an abscisic acid receptor stimulant raw drug and a preparation method thereof. The preparation method of the abscisic acid receptor stimulant raw drug comprises the following steps: adding quinolinone and halogenated propane into N, N-dimethyl formamide, and performing alkylation reaction to generate N-propyl quinolinone by taking sodium hydride as a catalyst; adding N-propyl quinolinone into dichloromethane, then, adding fuming nitric acid, and performing nitratlon reaction to generate 7-nitryl-propyl quinolinone; adding 7-nitryl-N-propyl quinolinone into an organic solvent ethanol, then, adding hydrochloric acid and iron powder, and performing hydrogenation reduction reaction to generate 7-amino-N-propyl quinolinone; adding 7-amino-N-propyl quinolinone into an organic solvent acetonitrile, then, adding 4-methyl benzylsulfonyl chloride, performing condensation reaction to generate N-(2-carbonyl-1-propyl-1,2,3,4-4H-quinolinone-6-)-4-p-methyl sulfamide, namely a abscisic acid receptor stimulant by taking N, N-diisopropylethylamine as a catalyst. The method has a relatively high yield; the prepared abscisic acid receptor stimulant raw drug is free of an optical isomer, easy to purify and relatively low in cost.