2'-ЗАМЕЩЕННЫЕ 1,1'-БИФЕНИЛ-2-КАРБОНАМИДЫ, СПОСОБЫ ИХ ПОЛУЧЕНИЯ, ИХ ПРИМЕНЕНИЕ В КАЧЕСТВЕ ЛЕКАРСТВЕННОГО СРЕДСТВА, А ТАКЖЕ СОДЕРЖАЩИЕ ИХ ФАРМАЦЕВТИЧЕСКИЕ КОМПОЗИЦИИ

Изобретение относится к органической химии, в частности к соединениям формулы (I): где R(1), R(2), R(3), R(4), R(5), R(6), R(7), R(8), R(30) и R(31) имеют указанные в формуле изобретения значения, которые в высшей степени пригодны в качестве нового рода антиаритмических биологически активных веществ, в особенности для лечения и профилактики аритмий предсердий, как, например, мерцание предсердий (фибрилляция предсердий, AF) или трепетание предсердий (предсердные трепетания). 12 з.п. ф-лы, 1 табл.

СУЛЬФОНАМИДНЫЕ ИНГИБИТОРЫ HIY - АСПАРТИЛ-ПРОТЕАЗЫ, ФАРМАЦЕВТИЧЕСКАЯ КОМПОЗИЦИЯ, СПОСОБ ЛЕЧЕНИЯ, СПОСОБ ИДЕНТИФИКАЦИИ ИНГИБИТОРА

Изобретение относится к новому классу сульфонамидов, которые являются ингибиторами аспартил-протеазы формулы I. Изобретение относится к новому классу H1У аспартил-протеазных ингибиторов, отличающемуся специфическими структурными и физико-химическими характеристиками. Изобретение относится также к фармацевтическим композициям, содержащим эти соединения. Соединения и фармацевтические композиции изобретения особенно подходят для ингибирования Н1У-1 и Н1У-2 протеазной активности, и, соответственно, их можно с выгодой использовать в качестве вирусных агентов против Н1У-1 и Н1У-2 вирусов. Изобретение относится также к способам ингибирования активности Н1У аспартил-протеазы, за счет использования соединений настоящего изобретения, и способам скринирования соединений по их анти-HIУ активности. 5 с. и 21 з.п. ф-лы, 3 ил., 8 табл.

Способ получения замещенных 1-аминонафталин-5-сульфамидов

Изобретение касается производства замещенных 1-аминонафталин-5-сульфамидов, в частности получения соединений, содержащих в сульфамидной группе -NR R . где она представляет собой а) М(СН )С Н б) -NH(CH ) в) -NH(C Н Уг) -N-гек3 2 51 3 2 5 детектирующих групп субстратов для определения ферментативной активности протеаз. Цель - удешевление и упрощение процесса Его ведут реакцией хлористого тионила с 1-нитронафталин- 5-сульфокислотой в среде диметилформамида с последующим аминированием образующегося сульфохлорида соответствующим амином в среде органического растворителя (CCI , СН CI, бензола) или в двухфазной системе: толуол или бензол - водный раствор Na CO и восстановлением полученного продукта, например, в среде метанола в присутствии никеля Ренея или обработкой восстановителями Fe/HCI или SnCI /HCI. Эти условия позволяют получать изомерно чистые целевые продукты , пригодные непосредственно в указанном анализе протеаз, что дешевле и проще, чем в известном случае. 1 з п. ф-лы, 2 табл.

Полиаминные аналоги в качестве цитотоксических агентов

... 1. Цитотоксический полиаминный аналог, имеющий структуру R1-X-R2, где R1 и R2 - независимо Н или радикал, выбранный из группы, включающей прямой или разветвленный C1-10 алифатический, алициклический, одно- или многокольцевой ароматический, одно- или многокольцевой арил-замещенный алифатический, алифатически замещенный одно- или многокольцевой ароматический, одно- или многокольцевой гетероциклический, одно- или многокольцевой гетероциклически замещенный алифатический и алифатически замещенный ароматический, а также их галогенированные формы; Х - полиамин с двумя концевыми аминогруппами, -(CH2)3-NH- или -СН2-Ph-СН2-, при этом R1 и R2 - не являются одновременно незамещенными бензиловыми радикалами. 2. Аналог по п.1, отличающийся тем, что Х выбирают из группы, содержащей путресцин, спермидин и спермин. 3. Аналог по п.1, отличающийся тем, что Х является путресцином. 4. Аналог по п.3, отличающийся тем, что указанная структура представляет собой соединение, которое выбрано из группы, включающей ...

4-(Аренсульфамидо)- -ацетилбензолсульфамиды, проявляющие диуретическую активность

Способ получения сульфаниламида

Способ получения производных 3-алкил-4-сульфамоиланилина

Способ очистки динитроанилинов от нитрозаминов

Способ получения 2-аминометил- ( -оксиалкил/пирролидинов)

Способ получения производных сульфамилбензиламина или их солей

Инсектицид

SKIN-EQUIVALENT

VERFAHREN ZUR REINIGUNG VON NITROSAMINE ENTHALTENDEN DINITROANILINEN

ORTHOSUBSTITUIERTE ARYLAMIDE ZUR BEKÄMPFUNG VON WIRBELLOSEN SCHÄDLINGEN

Insectizide N'-substituierte-N-alkylcarbonyl-N'-acylhydrazine und N'-substituierte-N-acyl-N'-alkylcarbonyl hydrazine.

Sulfonamid inhibitoren von Hiv-aspartyl Protease

SUBSTITUIERTE BENZAMIDE, VERFAHREN ZU DEREN HERSTELLUNG UND DIESE VERBINDUNGEN ALS WIRKSTOFFE ENTHALTENDE PHARMAZEUTISCHE ZUBEREITUNGEN

AMINOSÄUREDERIVATE, DIESE VERBINDUNGEN ENTHALTENDE ARZNEIMITTEL UND VERFAHREN ZU IHRER HERSTELLUNG

PROCESS FOR PREPARING BENZAMIDES

... 1394563 Process for 2-alkoxy- or -alkenoxy- 4,5-substituted-benzamides SOC D'ETUDES SCIENTIFIQUES ET INDUSTRIELLES DE L'ILE-DE-FRANCE 29 May 1973 [1 June 1972 (2) 12 June 1972 3 April 1973] 25402/73 Heading C2C Compounds (I) in which R 1 is a hydrogen atom or a methyl group, Z is a C 1-4 alkyl radical or a C 2-4 alkenyl radical, X is a hydrogen atom or a nitro or acylamino group, Y is a hydrogen or halogen atom, or a group of formula SO 2 R 2 in which R 2 is an amino, monoalkylamino, dialkylamino, C 1-5 alkyl or halogenoalkyl group, n is 0, 1, 2 or 3, A is a radical of the formula in which R 3 and R 4 are identical or different alkyl groups or are joined to form a heterocycle with the nitrogen, or A is a heterocyclic radical (II) where R is C 1-4 alkyl or alkenyl and m is up to 4, are prepared by reacting a corresponding 2-alkoxy- or -alkenoxy-X,Y-substituted benzoic acid sequentially with an alkyl haloformate and H 2 N(CHR 1 ) n A. (I) can, if desired, be converted into acid addition or ...

ISOTHIOCYANATES

... 1422223 Heterocyclic isothiocyanates SOC D'ETUDES SCIENTIFIQUES ET INDUSTRIELLES DE L'ILE-DE-FRANCE 1 June 1973 [2 June 1972 5 April 1973] 32538/75 Divided out of 1422221 Heading C2C The invention comprises compounds of Formula I in which m is 0, 1, 2, 3 or 4; n is 0, 1 or 2; p is 0 or 1; q is 0, 1 or 2, n + p + q is 0, 1, 2 or 3 and R is a C 1-4 alkyl or C 2-4 alkenyl radical which may be prepared by reaction of a compound of Formula II in which m, n, p, q and R are as defined above, in a basic medium with a salt of a metal whose sulphide is insoluble in the reaction medium (e.g. lead acetate) or with an ester of a haloformic acid (e.g. ethyl chloroformate).

TRIFLUOROMETHYL-SUBSTITUTED AMINOARYL-SULPHONYL COMPOUNDS

Trifluoromethylarylsulphonic acids, -sulphonamides and -sulphones of the formula I in which the substituents are defined in Claim 1, are prepared. These compounds are obtained by a chemically original process in which corresponding o- or p-haloarylsulphonyl compounds are reacted in non-aqueous solvents with ammonia under pressure and at elevated temperature. The said compounds can be used to prepare azo dyes by diazotisation and coupling to coupling components.

MANUFACTURE OF DIMETHYLAMINOBENZENE COMPOUNDS

... 1507320 Manufacture of dimethylaminobenzenes BASF AG 8 Aug 1975 [10 Aug 1974 16 Nov 1974] 33141/75 Addition to 1462258 Heading C2C The invention comprises a process for the manufacture of compounds of Formula I wherein individual radicals R1, R2, R3 are independently halogen, optionally substituted aliphatic or aromatic hydrocarbon radical -SO 3 R4, SO 2 N(R4) 2 , SO 2 R4, SO 2 NHCOR4, OR4, COR4, NHCOR4 wherein R4 is an optionally substituted aliphatic hydrocarbon radical, and the individual radicals R2 and R3 may also be independently hydrogen, phenoxy or -CO 2 R5, R5 being an optionally substituted aliphatic, cycloaliphatic, araliphatic or aromatic hydrocarbon radical, and adjacent radicals R3 or R1 and an adjacent radical R3 may also, together with the two carbon atoms linking them, form a fused heterocyclic radical, wherein ...

Substituted benzenesulfonamide derivatives as prodrugs of cox-2 inhibitors

Novel 2-cyano-3-(halo)alkoxy-benzenesulfonamide compounds for combating animal pests

Azabicyclic carbamoyloxy mutilin derivatives for antibacterial use.

Compounds of formula (3), and pharmaceutically acceptable salts and derivatives thereof: in which: R.1 is vinyl or ethyl; and R2 is a group R3, R4CH2~, or R5R6C=CH-; wherein each of R3 and R4 is an azabicyclic ring system or R5 and R^ together with the carbon atom to which they are attached form an azabicyclic ring system, are useful in the prevention and treatment of microbial infections.

Peptide deformylase inhibitors

Substituted benzenesulfonamide derivatives as products of COX-2 inhibitors.

Prodrugs of COX-2 inhibitors are described as beina useful in treating inflammation and inflammation-related disorders.

Novel sulfonamide inhibitors aspartyl protease.

The present invention relates to a novel class of sulfonamides which are aspartyl protease inhibitors. In one embodiment, this invention relates to a novel class of hiv aspartyl protease inhibitors characterized by specific structural and characterized by specific structural and physicochemical features this invention also relates to pharmaceutical compositions comprising these compounds. The compounds and pharmaceutical compositions of this invention are particularly well suited for inhibiting hiv-1 and hiv-2 protease activity and consequently, may be advantageously used as anti-viral agents against the hiv-1 and hiv-2 viruses. This invention also relates to methods for inhibiting the activity of hiv aspartly protease using the compounds of this invention and methods for screening compounds for ant-hiv activity ...

Carbamoyloxy derivatives of mutiline and their use as antibacterials.

Derivatives of mutiline of formula (1a)and pharmaceutically acceptable salts and derivatives thereof, in which r1 is ethyl or vinyl, y is a carbamoyloxy group, which the n-atom is unsubstituted, or mono- or di-substituted, are useful in the treatment of bacterial infections.

Novel compounds

NOVEL SULFONAMIDE INHIBITORS OF ASPARTYL PROTEASE

IL-8 receptor antagonists.

The invention relates to novel hydroxy diphenylurea sulfonamides, compositions and intermediates thereof. The hydroxy diphenylurea sulfonamides are useful in the treatment of disease states mediated by the chemokine, interleukin-8.

Novel compounds.

Compounds of formula (1a)and pharmaceutically acceptable salts and derivativews thereof in which y is a carbamoyloxy group, in which the n-atom is unsubstituted, or mono- or di-substituted, are useful in the treatment of bacterial infections.

Substituted benzenesulfonamide derivatives as prodrugs of cox-2 inhibitors

Peptide deformylase inhibitors.

Novel 2-cyano-3-(halo)alkoxy-benzenesulfonamide compounds for combating animal pests

Novel 2-cyano-3-(halo)alkoxy-benzenesulfonamide compounds for combating animal pests

Carbamoyloxy derivatives of mutiline and their useas antibacterials.

Hydroxy diphenyl urea sulfonamides as IL-8 receptor antagonists.

Method of preparation of new benzenedisulfonamides substituted usable like anthelminthic.

Substituted benzenesulfonamide derivatives as prodrugs of cox-2 inhibitors

Anilinométhylenemalonitriles and their uses as insecticides and pesticides.

New substtitués benzamides, their derivatives and their method of preparation.

Peptide deformylase inhibitors.

Peptide deformylase inhibitors.

Carb moylo y der vativ s of utiline and their use as antibacterials

NOVEL SULFONAMIDE INHIBITORS OF ASPARTYL PROTEASE

Novel compounds

Novel compounds

Peptide deformylase inhibitors.

VERFAHREN ZUR HERSTELLUNG VON NEUEN 4-AMINOPHENOXY- ODER 4-AMINOPHENYLTHIO-3-AMINO-5-SULFAMOYL-BENZOESAUREN SOWIE DEREN NIEDERALKYLESTERN UND SALZEN

CONNECTIONS, FROM THE CONNECTION MANUFACTURE POLYMER AND THE POLYMER CONTAINING MIXTURE

PROCEDURE FOR the PRODUCTION OF NEW ONES 4-AMINOPHENOXY OR 4-AMINOPHENYLTHIO-3-AMINO-5-SULFAMOYL-BENZOESAUREN AS WELL AS OF THEM NIEDERALKYLESTERN AND SALTS

1-Ä (ADAMANTYL) ALKYLÜ-3 Ä (PYRIDINYL) ALKYLÜHARNSTOFF CONNECTIONS AS TNF .ALPHA HEMMER TO the TREATMENT OF AUTOCIMMUNE ILLNESSES

VERFAHREN ZUR HERSTELLUNG VON SULFAMYLBENZOESAUREN

Shut-off device

PROCEDURE FOR THE PRODUCTION OF SULFAMYLBENZOESAEUREN

MUSCARIN RECEPTOR ANTAGONIST.

INSECTIZIDE N' SUBSTITUTE N ALKYLCARBONYl N'ACYLHYDRAZINE AND N' SUBSTITUTE N ECYl N'ALKYLCARBONYL HYDRAZINE.

NEW SULPHONYL PHENYLALKYLAMINE ONE, PROCEDURE FOR YOUR PRODUCTION AS WELL AS DRUG.

POLYAMINE-SIMILAR AS CYTOTOXIC ACTIVE SUBSTANCES

2-AMINOALKYL-1,4-DIAMINOBENZOL-DERIVATE AND THESE CONNECTIONS ABSTENTION COLORING MEANS

GLUCAGON ANTAGONIST/INVERSE AGONISTEN

4-JOD-2 n (N-ALKYL-AMINOCARBONYL) - AMINOSULFONYL) - BENZOE ÄUREMETHYLESTER AND - DERIVATIVES AND PROCEDURES FOR THEIR PRODUCTION

ANTHRANILSÄURE DERIVATIVES

SULFONE AMIDE DERIVATIVES

SULFONAMIDE INHIBITORE OF HIV ASPARTYL PROTEASE

Derivatives of benzosulphonamides as inhibitors of the enzyme cyclo-oxygenase II

2'-substituted 1,1'-biphenyl-2-carbonamides, method for the production thereof, use thereof as a medicament and pharmaceutical preparations containing said compounds

Nitroaniline-based alkylating agents and their use as prodrugs

1-ARYL 2-AMINOMETHYL CYCLOPROPANE CARBOXYLATES

Acylated aminophenyl urea compounds, their preparation and their use as herbicides and plant-growth regulators

PEPTIDE DEFORMYLASE INHIBITORS

Methods for treating spinal cord injury

Described herein are methods and compositions for treating a spinal injury. Aspects of the invention relate to administering to a subject an agent that upmodulates KCC2. Another aspect of the invention relates to administering to a subject an agent that that reduces excitability of inhibitory interneurons. Compositions comprising these agents are additionally described herein.

1-ARYL 2-AMINOMETHYL CYCLOPROPANE CARBOXYLATES

Carbamoyloxy derivatives of mutiline and their use as antibacterials

Novel compounds and their use as positive ampa receptor modulators

N-PHENYLSULPHONYL - N:PYRIMIDINYL - AND - TRIAZINYL-UREAS

4-jod-2{n-(n-alkyl-aminocarbonyl)-aminosulfonyl}-benzoic acid methyl ester and derivatived thereof and method for their production

Sulfonamide inhibitors of hiv-aspartyl protease

HALOETHYL UREA COMPOUNDS AND THE USE THEREOF TO ATTENUATE, INHIBIT OR PREVENT CANCER CELL MIGRATION

PHENYL DERIVATIVES AND THEIR USE IN THE TREATMENT OF THROMBOEMBOLIC DISORDERS OR TUMOURS

Compounds of the formula (I) in which R1 is CN, or C(=NH)-NH2, CON(R3)2 or [C(R4)2]nN(R3)2, each of which is unsubstituted or monosubstituted by C(=O)R3, COOR3, or3 or by a conventional amino-protecting group, or W is -NR3CO-, - NR3COC(R4)2, NR3C(R4)2) or -C(R4)2NR3C(R4)2-, X is -C(R3)2-, -[C(R3)2]2-, - C(R3)2O- or -C(R3)2NR3, Y is alkylene, cycloalkylene, Het-diyl or Ar-diyl, T is OR3, N(R3)2, N(R3)2CON(R3)2, a monocyclic or bicyclic, saturated, unsaturated or aromatic heterocyclic radical having from 1 to 4 N, O and/sor S atoms which is unsubstituted or monosubstituted, disubstituted or trisubstituted, or a phenyl radical which is unsubstituted or monosubstituted, disubstituted or trisubstituted are inhibitors of coagulation factor Xa and can be employed for the prophylaxis and/or therapy of thromboembolic disorders and for the treatment of tumours.

TNF-.ALPHA. PRODUCTION INHIBITORS

A purpose of the present invention is to provide TNF-.alpha. production inhibitors being useful as therapeutic agents for autoimmune diseases such as rheumatoid arthritis. Novel compounds having the structure represented by the general formula [1] or salts thereof according to the present invention have excellent TNF-.alpha. production inhibitory activities, (see formula 1) wherein "A" is -(NR4)- , -(CR5R6)- or -O-, "B" is alkylene or alkenylene, R1, R2, R4, R5 and R6 are hydrogen, alkyl, alkenyl, adamantyl or the like, R3 is aryl or an unsaturated heterocycle, and "X" is oxygen or sulfer respectively.

SUBSTITUTED BENZAMIDES AND DERIVATIVES THEREOF

Novel benzamides are provided which correspond to the formula: in which A represents a hydrogen atom, a C1-5 alkyl group, or a C2-5 alkenyl group; X represents a hydrogen atom, a C1-5 alkoxy group, a C1-5 alkyl group, a C2-5 alkenyloxy group, or a C2-5 alkenyl group; Y represents a hydrogen atom, a halogen atom, a nitro group, a C1-5 alkyl group, a C1-5 alkoxy group, an amino group, a substituted amino group such as for example alkylamino, acylamino, benzylamino or alkoxycarbonylamino; Z represents a hydrogen atom, a halogen atom, a C1-5 alkoxy group, a C1-5 alkylsulphonyl group, a SO2NR1R2 group in which R1 and R2, which may be the same or different, are hydrogen or a lower C1-5 alkyl group, or form, together with the nitrogen atom to which they are attached, a heterocycle optionally containing another hetero atom; W represents an alkylene group with 1 to 4 carbon atoms which may form a straight or branched chain; B represents a group NR1R2 in which R1 is a C1-5 alkyl group, R2 is a C1 ...

HALOETHYL UREA COMPOUNDS AND THEIR USE TO ATTENUATE, INHIBIT OR PREVENT NON-CANCEROUS PATHOGENIC CELLULAR PROLIFERATION AND DISEASES ASSOCIATED THEREWITH

DINITROANILINE PURIFICATION WITH BROMINE AND CHLORINE

3,4-DI-SUBSTITUTED CYCLOBUTENE-1,2-DIONES AS CXC-CHEMOKINE RECEPTOR LIGANDS

Disclosed are novel compounds of the formula (I)or a pharmaceutically acceptable salt or solvate thereof. Also disclosed is the treatment of chemokine-mediated diseases using compounds of the formula (II) ...

4-ARYLAMINO, 4-ARYLOXY, AND 4-ARYLTHIO DIARYLAMINES AND DERIVATIVES THEREOF AS SELECTIVE MEK INHIBITORS

The invention provides compounds of formula (II), wherein Ar, R3, R4, R5, R6, R7, R8 and W have the meanings given in the description. They are selective MEK inhibitors.

PHENYLHYDRAZONES, THE MANUFACTURE THEREOF AND THERAPEUTIC AND COSMETIC COMPOSITIONS PREPARED THEREFROM

A Phenylhydrazone of formula I: in which R1, R2, and R3 are independently of one another hydrogen, halogen, C1-C4-alkyl, hydroxyl, C1-C4-alkoxy or acetoxy, R4 is hydrogen, hydroxyl, tert.-butyl, C1-C6-alkoxy or C2- C6-alkoxyalkyl, R5 is hydrogen or C1-C4-alkyl, or R4 and R5 together form a ring which is -C(CH3)2-A-C(CH3)2-(where A is -CH2CH2-, -CH(CH3)-, -CH2C(O)-or-CH2CHOH-) or is -(CH2)3C(CH3)2-, -OCH2CH2C(CH3)2-, -C(CH3)2CH(CH3)CH2C(CH3)2- or -NHC(O)CH2C(CH3)2-, where R4 and R5 together form a ring of the type specified or R4 is branched C4-C6-alkoxy or branched C4-C6-alkoxyalkyl when R1, R2 and R3 are each hydrogen, R6 is hydrogen, methyl, ethyl or cyclopropyl, m and n are different and denote 0 or 1, X is hydrogen, nitro, methoxy or nitrile, a sulfonic acid radical or -CONR7 OR7, -CO2R7, -PO(OR8)2, -S(O)n R8 where n is 0,1 or 2, -SO2-NR9R10 or -CONR9R10, where R7 is hydrogen, C1-C3-alkyl or phenyl, which may or may not be substituted by one or two amino, C1-C4-acylamino, C1-C4- alkyl ...

Naphthyloxazolidone Derivatives

ALKYLIDENEHYDRAZINOPHENYLSULFONYLUREAS, PROCESSES FOR THEIR PREPARATION AND THEIR USE AS HERBICIDES AND PLANT GROWTH REGULATORS

Alkylidenehydrazinophenylsulfonylureas, processes for their preparation and their use as herbicides and plant growth regulators Compounds of the formula (I) and salts thereof (see formula I) in which R1 to R6, W, X, Y and Z are defined as in claim 1, have herbicidal or plant growth-regulatory properties. They can be prepared by processes analogous to known processes (cf. claim 5), in some cases via novel intermediate products (cf. formula II): (see formula II) ...

SUBSTITUTED BENZENESULFONAMIDE DERIVATIVES AS PRODRUGS OF COX-2 INHIBITORS

Prodrugs of COX-2 inhibitors of formula (I) are described as being useful in treating inflammation and inflammation-related disorders wherein A is a ring substituent selected from partially unsaturated heterocyclyl, heteroaryl, cycloalkenyl and aryl, wherein A is optionally substituted at a substitutable position with one or more radicals selected from alkylcarbonyl, formyl, halo, alkyl, haloalkyl, oxo, cyano, nitro, carboxyl, alkoxy, aminocarbonyl, alkoxycarbonyl, carboxyalkyl, cyanoalkyl, hydroxyalkyl, haloalkylsulfonyloxy, alkoxyalkyloxyalkyl, carboxyalkoxyalkyl, cycloalkylalkyl, alkenyl, alkynyl, heterocyclyloxy, alkylthio, cycloalkyl, aryl, heterocyclyl, cycloalkenyl, aralkyl, heterocyclylalkyl, alkylthioalkyl, arylcarbonyl, aralkylcarbonyl, aralkenyl, alkoxyalkyl, arylthioalkyl, aryloxyalkyl, aralkylthioalkyl, aralkoxyalkyl, alkoxycarbonylalkyl, aminocarbonylalkyl, alkylaminocarbonyl, Narylaminocarbonyl, N-alkyl-N-arylaminocarbonyl, alkylaminocarbonylalkyl, alkylamino, N-arylamino ...

TETRALINES

Compounds of formula (I) wherein R1 and R2, independently, are hydrogen (C1-4)alkyl, (C1-4)alkoxy, (C1-4)alkylthio, halogen, trifluoromethyl, trifluoromethoxy, cyano, (C2-5)alkanoyl, (C1-4)alkylsulfonyl or sulfamoyl; R3 is hydrogen, hydroxy, (C1-4)alkyl, (C1-4)alkoxy, halogen, cyano, (C2-5)alkanoyl, carbamoyl, (C1-4)alkylsulfonyloxy or trifluoromethylsulfonyloxy; and R4 and R5, independently, are hydrogen, (C1-4)alkyl, hydroxy(C2-4)alkyl or phenyl(C1-4)alkyl, or form together with the nitrogen atom to which they are attached a pyrrolidinyl, piperidino or piperazinyl group, in free base or acid addition salt form. Compounds according to formula (1) are useful in the treatment of epilepsy, stroke and brain or spinal trauma.

SOLUBLE COMBINATORIAL LIBRARIES

The present invention relates to novel soluble combinatorial libraries, comprising a soluble phase in solution attached to a core molecule, and allowing the improved high-yield and efficient production of soluble combinatorial libraries. Some specific examples of the soluble combinatorial libraries claimed herein comprise one or more of the following: amino acids, .alpha.-azetide amino acids, triazine dione molecules, .gamma.-lactamtide molecules, .delta.-lactamthiotide molecules, .beta.-lactam nucleus containing molecules, lycoramine alkaloid nucleus containing molecules, and .beta.blocker nucleus molecules. Further, a split synthesis technique for generating librairies of combinatorial molecules employs a biphasic macromolecular support which is soluble during the pooling, splitting, and coupling steps but which is insoluble during the washing step. The use of a biphasic macromolecular support in its soluble phase significantly enhances the efficiency and performance of the pooling, splitting ...

ANALOGS AND PRODRUGS OF BUMETANIDE; COMPOSITIONS AND METHODS OF USE

Novel analogs and prodrugs of the loop diuretic bumetanide are described. Pharmaceutical compositions containing bumetanide analogs and prodrugs are also described. These analogs and prodrugs are particularly useful for the treatment and/or prophylaxis of conditions that involve the NKCC cotransporter family (NKCC1 and NKCC2), or the KCC cotransporter family (KCC1, KCC2, KCC3, KCC4), or GABAa receptors. Such conditions include, but are not limited to anxiety disorders, epilepsy, migraine, non-epileptic seizures, sleep disorders, obesity, eating disorders, autism, depression, edema, glaucoma, stroke, ischemia, neuropathic pain, addictive disorders, schizophrenia, psychosis, and tinnitus. 1. A compound comprising an analog or prodrug of bumetanide.3. A compound of claim 1 , comprising a 5-amido or 5-keto bumetanide derivative in which the 5-ester has been replaced by either a ketone or an amide.9. A method for the treatment and/or prophylaxis of a neurological or psychiatric disorder comprising administering a composition having one of formulas I-VI disclosed herein.10. The method of claim 9 , wherein the neurological or psychiatric disorder is selected from the group consisting of: anxiety disorders (including posttraumatic stress disorder claim 9 , generalized anxiety disorder claim 9 , panic disorder claim 9 , obsessive compulsive disorder claim 9 , specific phobia) claim 9 , epilepsy claim 9 , migraine claim 9 , seizure disorders and non-epileptic seizures claim 9 , sleep disorders claim 9 , obesity claim 9 , eating disorders claim 9 , autism claim 9 , depression claim 9 , edema claim 9 , glaucoma claim 9 , stroke claim 9 , ischemia claim 9 , neuropathic pain claim 9 , addictive disorders claim 9 , schizophrenia claim 9 , psychosis claim 9 , and tinnitus.11. The method of claim 9 , comprising administering the composition following the onset of symptoms.12. The method of claim 9 , comprising administering the composition prophylactically prior to the onset of ...

DEUTERATED N-BUTYL BUMETANIDE

The present invention provides a compound of Formula I: 2. The compound of claim 1 , wherein Ris OH.3. The compound of wherein Yand Yare the same; Yand Yare the same; Yand Yare the same; and Yand Yare the same.4. The compound of claim 1 , wherein Yis hydrogen or deuterium; Yis hydrogen or deuterium; and Yand Yare each deuterium.5. The compound of claim 1 , wherein Yand Yare each deuterium.6. The compound of claim 1 , wherein Yand Yare each deuterium.7. The compound of claim 1 , wherein Yand Yare each deuterium.8. The compound of claim 1 , wherein Yis hydrogen or deuterium; Yis hydrogen or deuterium; Yis hydrogen or deuterium; and Yand Yare each deuterium.9. The compound of wherein Yand Yare each deuterium.10. The compound of claim 8 , wherein Yand Yare each deuterium.11. The compound of claim 1 , wherein Yis hydrogen or deuterium; Yis hydrogen or deuterium; and Yand Yare each deuterium.12. The compound of claim 1 , wherein Yis hydrogen or deuterium; Yis hydrogen or deuterium; and Yand Yare each deuterium.13. The compound of wherein Yand Yare each deuterium.14. The compound of claim 1 , wherein any atom not designated as deuterium is present at its natural isotopic abundance.20. A pharmaceutical composition comprising a compound of or a pharmaceutically acceptable salt thereof; and a pharmaceutically acceptable carrier.21. A method of modulating a GABAreceptor in a cell comprising contacting the cell with a composition of .22. A method of treating a disease or condition selected from the group consisting of epilepsy claim 20 , neuropathic pain claim 20 , nociceptive pain claim 20 , migraine claim 20 , addictive disorders claim 20 , Alzheimer's Disease claim 20 , anxiety disorders claim 20 , ascites claim 20 , autism claim 20 , bipolar disorder claim 20 , cancer claim 20 , depression claim 20 , endothelial corneal dystrophy claim 20 , edema claim 20 , glaucoma claim 20 , Huntington's Disease claim 20 , insomnia claim 20 , ischemia claim 20 , ocular diseases claim 20 , ...

BUMETANIDE ANALOGS, COMPOSITIONS AND METHODS OF USE

The present invention provides bumetanide, analogs and compositions comprising such analogs. The present invention also provides pharmaceutical compositions containing these bumetanide, analogs and methods for their use. These analogs are particularly useful for the treatment and/or prophylaxis of conditions that involve the NaKCl co-transporter or GABAreceptor including but not limited to addictive disorders, Alzheimer's Disease, anxiety disorders, ascites, autism, bipolar disorder, cancer, depression, endothelial corneal dystrophy, edema, epilepsy, glaucoma. Huntington's Disease, insomnia, ischemia, migraine, migraine with aura, neuropathic pain, nociceptive neuralgia, nociceptive pain, ocular diseases, pain, Parkinson's disease, personality disorders, postherpetic neuralgia, psychosis, schizophrenia, seizure disorders, tinnitus, and withdrawal syndromes. 1191-. (canceled)192. A compound comprising an N-amide analog of bumetanide.193. The compound of selected from the group consisting of: bumetanide N-morpholinoamide; bumetanide N-morpholinylthioamide; bumetanide N-tetrahydrooxazolythioamide; bumetanide N-tetrahydroisoxazolythioamide; bumetanide N-thiomnorpholinyhthioamide; bumetanide N-piperazinylthioamide and analogs; bumetanide N-tetrahydropyrimidinylthioamnide and analogs; bumetanide N-terahydropyridazinylthioamide and analogs; bumetanide N-4-piperadonyltioamide; bumetanide N-tetrahydroimidazolythioamide and analogs; bumetanide N-pyrazolidinylthioamide and analogs; bumetanide N-thiazolidinylthioamimde; bumetanide N-isothiazolidinylthioamide; bumetanide N-cis-2 claim 192 ,6-dimethylmorpholinylthioamide; bumetanide N-trans-2 claim 192 ,6dimethylmorpholinylthioamide; bumetanide N-cis-2 claim 192 ,6-dimethylthiomorpholinylthioamide; bumetanide N-trans-2 claim 192 ,6-dimethylthiomiorpholinyithxioamide; bumetanide N-3-methylpiperazinylthioamide and analogs (racemate claim 192 , R- and S-enantiomers); bumetanide N-3 claim 192 ,3-dimethylpiperazinylthioamide and ...

3-(BENZYLAMINO)-4-(CYCLOHEXYLAMINO)-N-(2-(PIPERAZIN-1-YL)ETHYL)BENZENESULFONAMIDE DERIVATIVES AND RELATED FERROSTATIN-1 ANALOGUES AS CELL DEATH INHIBITORS FOR TREATING E.G. STROKE

The present invention relates to 3-(benzylamino)-4-(cyclohexylamino)-N-(2-(piperazin-1-yl)ethyl)benzenesulfonamide derivatives and related ferrostatin-1 (Fer-1) analogues as cell death inhibitors by inhibition of ferroptosis and/or oxytosis for the treatment of stroke, myocardial infarction, diabetes, sepsis, the prevention of transplant rejection, neurodegenerative diseases including Alzheimer's disease, Parkinson's disease, amyotrophic lateral sclerosis, multiple sclerosis, Huntington's disease, dementia with Lewy bodies and Friedreich's ataxia. The present invention further relates to pharmaceutical compositions of these compounds and discloses methods for making the compounds and the corresponding intermediate. 16-. (canceled)8. A compound according to claim 7 , wherein R1 or R2 is a C1-C4-alkyl pyridinyl.9. A compound according to claim 7 , selected from the group consisting of 3-amino-4-(cyclohexylamino)-N-(2-(4-methylpiperazin-1-yl)ethyl)b enzenesulfonamide claim 7 , 3-amino-4-(cyclohexylamino)-N-(2-morpholino-ethyl)benzenesulfonamide claim 7 , 3-amino-4-(cyclohexylamino)-N-(2-(piperazin-1-yl)ethyl)-benzenesulfonamide claim 7 , 3-(benzylamino)-4-(cyclohexylamino)-N-(2-(4-methylpiperazin-1-yl)ethyl)benzenesulfonamide claim 7 , 4-(cyclohexylamino)-N-(2-(4-methylpiperazin-1-yl)ethyl)-3-((pyridin-4-ylmethyl)amino)benzenesulfonamide claim 7 , 4-(cyclohexylamino)-N-(2-morpholinoethyl)-3-((pyridin-4-ylmethyl)amino)benzenesulfonamide claim 7 , 4-(cyclohexylamino)-N-(2-(piperazin-1-yl)ethyl)-3-((pyridin-4-ylmethyl)amino)benzenesulfonamide hydrochloride claim 7 , 3-(benzylamino)-4-(cyclohexylamino)-N-(2-morpholinoethyl)benzenesulfonamide and 3-(benzylamino)-4-(cyclohexylamino)-N-(2-(piperazin-1-yl)ethyl)benzenesulfonamide hydrochloride.10. A medicament comprising a compound of or a stereoisomer claim 7 , a tautomer claim 7 , an N-oxide claim 7 , a hydrate claim 7 , a solvate claim 7 , or a salt thereof claim 7 , particularly a pharmaceutically acceptable salt thereof ...

Method of fighting unwanted plant growth

1389479 Substituted 2,6-dinitroaniline compounds AMERICAN CYANAMID CO 6 July 1972 [25 Aug 1971] 31784/72 Heading C2C Substituted 2,6-dinitroaniline compounds of the general formula: in which R is 1-ethylbutyl, 1-ethylpropyl, 1- methylpropyl or 1-methylbutyl are prepared by reacting a compound of the general formula: with an amine or the formula RNH 2 . The compounds have herbicidal properties.

METHOD FOR PRODUCING SOLUBLE STREPTOCIDE

А 2016102981 ко РОССИЙСКАЯ ФЕДЕРАЦИЯ до ах сад ща ДРРАН 19) у п? заза ча за4( А << “<® & < (50) МПК Аб1К 31/63 (2006.01) С07С 30300 (2006.0Т) С07С 311/39 (2006.01) ФЕДЕРАЛЬНАЯ СЛУЖБА ПО ИНТЕЛЛЕКТУАЛЬНОЙ СОБСТВЕННОСТИ (12) ЗАЯВКА НА ИЗОБРЕТЕНИЕ (21)(22) Заявка: 2016102981, 29.01.2016 (71) Заявитель(и): Открытое акционерное общество "Ирбитский а полачи заявки: 29.01.2016 Ко Оариадевтическ Заводе СВ | (72) Автор(ы): (43) Дата публикации заявки: 07.08.2017 Бюл. № 22 Солодухина Людмила Александровна (ВП), Адрес для переписки: Абросимова Людмила Александровна (КП) 105082, Москва, а/я 111, ООО Юридическая фирма "Ломский и партнеры", Ломскому Сергею Михайловичу (54) СПОСОБ ПОЛУЧЕНИЯ СТРЕПТОЦИДА РАСТВОРИМОГО (57) Формула изобретения Способ получения стрептоцида растворимого, по которому растворяют пиросульфит натрия в воде, добавляют формалин, при РН 8,0-10,0 реакционной массы добавляют уголь активный и массу выдерживают при перемешивании и температуре 55+10°С в течение 1-1,5 часов, добавляют воду и стрептоцид, реакционную массу перемешивают в течение, постепенно добавляют серную кислоту до рН реакционной массы 3,0-4,0 с последующим нагревом и выдержкой загружают уголь активный, рН реакционной массы серной кислотой доводят до 3,0-4,5, загружают подогретый до температуры 50=10°С изопропиловый спирт в количестве, реакционную массу перемешивают и выдерживают при периодическом перемешивании, по окончании выдержки реакционная масса охлаждается, промывается изопропиловым спиртом, сушится и измельчается. Стр.: 1 па 86$01910Сс У

Patent FR2151415A5

Antagonists of RF-amide neuropeptides

Disclosed are compounds having the formula: where R 1 =H, C 1 -C 6 alkyl, cycloalkyl, R 2 =H, C 1 -C 6 alkyl, cycloalkyl W=C n H 2n-m —NH (n=1-6, m=0, 2, or 4), Z=CONR 8 (CH 2 ) n , CONR 8 (CH 2 ) n CO, P(CH 3 )OCHR 8 OCOR 9 , SO 2 , SO 2 (CH 2 ) n , SO 2 (CH 2 ) n CO, SO 2 NR 8 (CH 2 ) n , SO 2 NR 8 (CH 2 ) n CO, n=1-4 R 4 =H, (CH 2 ) n OH, (CH 2 ) n OCOR 10 , (CH 2 ) n NR 10 R 11 , (CH 2 ) n CONR 10 R 11 , n=0-4 R 5 =H, (CH 2 ) n NR 12 R 13 , n=0-4 R 6 =H, (CH 2 ) n NR 14 R 15 , n=0-4 R 7 =H, C 1 -C 6 alkyl, cycloalkyl; R 8 =H, C 1 -C 6 alkyl, cycloalkyl; R 9 =H, C 1 -C 6 alkyl, cycloalkyl; R 10 =H, C 1 -C 6 alkyl, cycloalkyl; R 11 =H, C 1 -C 6 alkyl, cycloalkyl; R 12 =H, C 1 -C 6 alkyl, cycloalkyl; R 13 =H, C 1 -C 6 alkyl, cycloalkyl; R 14 =H, C 1 -C 6 alkyl, cycloalkyl; R 15 =H, C 1 -C 6 alkyl, cycloalkyl Dashed lines: optional; conformational constraint by (CH 2 ) n , n=1-3, R′=H or O(═) as well as pharmaceuticals compositions and methods for the treatment of opiate addiction, opiate dependence, opiate tolerance, opiate related abstinence syndrome, nicotine addition and obesity based thereon.

2,6-dinitroaniline herbicides

Method for obtaining a streptocide soluble

FIELD: medicine; pharmacology.SUBSTANCE: present invention relates to the field of pharmacology and discloses a process for the preparation of a soluble streptocide. Method is characterized in that sodium pyrosulphite is dissolved in water, formalin is added, at pH 8.0-10.0 of the reaction mass, active carbon is added and the mass is kept with stirring for 1-1.5 hours, water and streptocide are added, the reaction mass is stirred, sulfuric acid is gradually added until the reaction mass is reached pH of 3.0-4.0, followed by heating and soaking, active carbon is loaded, the pH of the reaction mixture with sulfuric acid is adjusted to 3.0-4.5, preheated isopropyl alcohol is charged, the reaction mass is stirred and kept under intermittent stirring, after the end of aging, the reaction mass is cooled, washed with isopropyl alcohol, dried and milled.EFFECT: method makes it possible to obtain a product of compendial grade and can be used in the pharmaceutical industry for the manufacture of ready-to-use combined medicines in the form of solutions, aerosols, sprays, liniments containing streptocide soluble.1 cl РОССИЙСКАЯ ФЕДЕРАЦИЯ (19) RU (11) (13) 2 663 071 C2 (51) МПК A61K 31/63 (2006.01) C07C 303/00 (2006.01) C07C 311/39 (2006.01) ФЕДЕРАЛЬНАЯ СЛУЖБА ПО ИНТЕЛЛЕКТУАЛЬНОЙ СОБСТВЕННОСТИ (12) ОПИСАНИЕ ИЗОБРЕТЕНИЯ К ПАТЕНТУ (52) СПК A61K 31/63 (2006.01); C07C 303/00 (2006.01); C07C 311/39 (2006.01) (21)(22) Заявка: 2016102981, 29.01.2016 (24) Дата начала отсчета срока действия патента: (73) Патентообладатель(и): Открытое акционерное общество "Ирбитский химико-фармацевтический завод" (RU) Дата регистрации: 01.08.2018 (56) Список документов, цитированных в отчете о поиске: Пассет Б.В., Воробьева В.Я. (43) Дата публикации заявки: 07.08.2017 Бюл. № 22 (45) Опубликовано: 01.08.2018 Бюл. № 22 2 6 6 3 0 7 1 R U (54) СПОСОБ ПОЛУЧЕНИЯ СТРЕПТОЦИДА РАСТВОРИМОГО (57) Реферат: Настоящее изобретение относится к области кислотой доводят до 3,0-4,5, загружают фармакологии и раскрывает ...

The method and P-aminobenzene-sulfonamide of a kind of antifebrin synthesis P-aminobenzene-sulfonamide rapidly and efficiently

一种快速高效的乙酰苯胺合成对氨基苯磺酰胺的方法及对氨基苯磺酰胺，属于对氨基苯磺酰胺合成领域。方法包括：将乙酰苯胺、氯磺酸于四氯化碳中混合并加热至50‑60℃磺化反应40‑60min得到磺化液。在紫外光的照射作用下，将磺化液与二氯亚砜混合的混合液加热至70‑80℃氯化反应40‑60min得到氯化液，氯化反应中将液料进行雾化。将氯化液结晶得到的对乙酰氨基苯磺酰氯依次进行胺化反应及水解反应。其操作方便、合成效率高。对氨基苯磺酰胺根据上述的方法制得，生产快、纯度高。

METHOD FOR THE PRODUCTION OF NEW 2- -BENZYLIDENAMINO-5-SULFAMYL-BENZAMIDES AND THEIR POTASSIUM SALTS

METHOD FOR PRODUCING NEW 2-BENZYLIDENAMINO-5-SULFAMYL-BENZAMIDES AND THEIR POTASSIUM SALTS

一种功能性焦糖及其作为阻燃整理剂的应用

本发明涉及一种功能性焦糖及其作为阻燃整理剂的应用，该功能性焦糖是由小分子糖和物质A在水中混合均匀后，在碱性条件下发生美拉德反应得到；其中，小分子糖为葡萄糖、蔗糖和果糖中的一种或多种，物质A为牛磺酸和/或磺胺。该功能性焦糖作为阻燃整理剂的应用过程是将功能性焦糖作为阻燃整理剂对纤维制品进行染整加工；所述纤维制品中的纤维为聚酰胺纤维。染整加工后的纤维制品的烟密度为5～12，且染整加工后的纤维制品的阻燃等级为V‑0级，且耐水洗。本发明中的功能性焦糖，用于聚酰胺织物的整理后，阻燃性能良好，符合V‑0级的标准，而且具有较强的耐水洗性能。

一种可生产多种染料中间体的生产线

本发明属于染料中间体制备技术领域，具体地说，涉及一种可生产多种染料中间体的生产线。所述的可生产多种染料中间体的生产线上顺序连接有氯磺化釜、氨化釜、氨保釜、水解釜、酸化釜、还原釜、中和釜和调浆釜。本发明在中和釜后增加调浆釜，采用输送泵将液体浆料直接输送到生产车间，减轻了工人的劳动强度。本发明的生产线具备生产多种染料中间体的能力。通过优化，大幅降低固定资产投入上千万元，减少设备闲置，提高设备及土地利用率，且由于反应釜体积扩大，瞬间产能大幅提高，满足了瞬息万变的市场需求。并且在设备台数减少的同时最大程度实现自动化控制，提高生产效率和产品质量，降低劳动强度，降低人工成本。

一种功能性焦糖及其作为阻燃整理剂的应用

本发明涉及一种功能性焦糖及其作为阻燃整理剂的应用，该功能性焦糖是由小分子糖和物质A在水中混合均匀后，在碱性条件下发生美拉德反应得到；其中，小分子糖为葡萄糖、蔗糖和果糖中的一种或多种，物质A为牛磺酸和/或磺胺。该功能性焦糖作为阻燃整理剂的应用过程是将功能性焦糖作为阻燃整理剂对纤维制品进行染整加工；所述纤维制品中的纤维为聚酰胺纤维。染整加工后的纤维制品的烟密度为5～12，且染整加工后的纤维制品的阻燃等级为V‑0级，且耐水洗。本发明中的功能性焦糖，用于聚酰胺织物的整理后，阻燃性能良好，符合V‑0级的标准，而且具有较强的耐水洗性能。

一种可生产多种染料中间体的生产线

本发明属于染料中间体制备技术领域，具体地说，涉及一种可生产多种染料中间体的生产线。所述的可生产多种染料中间体的生产线上顺序连接有氯磺化釜、氨化釜、氨保釜、水解釜、酸化釜、还原釜、中和釜和调浆釜。本发明在中和釜后增加调浆釜，采用输送泵将液体浆料直接输送到生产车间，减轻了工人的劳动强度。本发明的生产线具备生产多种染料中间体的能力。通过优化，大幅降低固定资产投入上千万元，减少设备闲置，提高设备及土地利用率，且由于反应釜体积扩大，瞬间产能大幅提高，满足了瞬息万变的市场需求。并且在设备台数减少的同时最大程度实现自动化控制，提高生产效率和产品质量，降低劳动强度，降低人工成本。

신규 단실 형광 화합물 라이브러리의 합성 방법과 이를 이용한 살아있는 세포 이미징 방법

본 발명은 단실 유도체의 새로운 용도에 대한 것으로, 구체적으로 단실 유도체가 살아있는 세포를 이미징하는데 유용하게 활용될 수 있음을 밝힌 것이다. 본 발명의 제조 방법 및 이를 통해 제조된 다양한 단실 유도체는 세포와 접촉시 세포내에 위치 하므로, 이를 통하여 세포 이미징에 유용하게 활용될 수 있다. 따라서, 이러한 분자는 살아있는 세포의 이미징을 가능하게 하므로, 다양한 연구 및 산업적인 용도로 활용될 수 있다.

Method of synthesizing novel fluorescent probe library of dansyl scaffold and method of imaging live cells by using the same

Provided is a novel use of adansyl derivative, and, in particular, a dansyl derivative that may be effectively used in imaging live cells. A preparation method of the present invention and various types of dansyl derivatives prepared by using the method may be effectively used in cell imaging since the dansyl derivatives are located in cells when the dansyl derivatives contact with the cells. Thus, the dansyl derivatives enable imaging of live cells and thus may be used in various studies and industrial fields.

신규 단실 형광 화합물 라이브러리의 합성 방법과 이를 이용한 살아있는 세포 이미징 방법

본 발명은 단실 유도체의 새로운 용도에 대한 것으로, 구체적으로 단실 유도체가 살아있는 세포를 이미징하는데 유용하게 활용될 수 있음을 밝힌 것이다. 본 발명의 제조 방법 및 이를 통해 제조된 다양한 단실 유도체는 세포와 접촉시 세포내에 위치 하므로, 이를 통하여 세포 이미징에 유용하게 활용될 수 있다. 따라서, 이러한 분자는 살아있는 세포의 이미징을 가능하게 하므로, 다양한 연구 및 산업적인 용도로 활용될 수 있다.

一种塞来昔布中间体对肼基苯磺酰胺盐酸盐的合成方法

本发明涉及一种塞来昔布中间体对肼基苯磺酰胺盐酸盐的合成方法，属于药物中间体合成技术领域，具体合成工艺是以稀盐酸为溶剂先泵入到动态管式反应器中，然后将对氨基苯磺酰胺固体、亚硝酸钠溶液分别加入到动态管式反应器中进行重氮化反应，反应完将反应液转入到亚硫酸钠水溶液中还原，后经过酸化、除杂、析晶后得到对肼基苯磺酰胺盐酸盐纯品。该方法安全环保，操作简便，反应时间短，产品纯度高。

一种塞来昔布中间体对肼基苯磺酰胺盐酸盐的合成方法

本发明涉及一种塞来昔布中间体对肼基苯磺酰胺盐酸盐的合成方法，属于药物中间体合成技术领域，具体合成工艺是以稀盐酸为溶剂先泵入到动态管式反应器中，然后将对氨基苯磺酰胺固体、亚硝酸钠溶液分别加入到动态管式反应器中进行重氮化反应，反应完将反应液转入到亚硫酸钠水溶液中还原，后经过酸化、除杂、析晶后得到对肼基苯磺酰胺盐酸盐纯品。该方法安全环保，操作简便，反应时间短，产品纯度高。

Flourescence labeling reagents and uses thereof

Solid phase fluorescent labeling reagents (SPR) are described that simultaneously capture and label analytes, and then efficiently release the labeled-analytes under mild conditions (SCaLER).

塞来昔布的有关物质及其制备方法和应用

本发明公开了塞来昔布的有关物质及其制备方法和应用，属于药物合成技术领域，解决了现有技术中尚未有对塞来昔布的N‑亚硝基化合物有关物质进行研究的问题。本发明的塞来昔布的有关物质结构如式I所示，本发明还公开了该有关物质的制备方法，及其在检测塞来昔布中间体、原料药和/或制剂中的应用。本发明首次提供了塞来昔布的N‑亚硝基化合物有关物质及制备方法，为塞来昔布的质量研究、标准研究、稳定性研究、药品不良反应的机制研究提供了基础；同时，为塞来昔布的生产、包装、储存、运输及应用条件的选择提供依据。

一种功能性焦糖及其作为阻燃整理剂的应用

本发明涉及一种功能性焦糖及其作为阻燃整理剂的应用，该功能性焦糖是由小分子糖和物质A在水中混合均匀后，在碱性条件下发生美拉德反应得到；其中，小分子糖为葡萄糖、蔗糖和果糖中的一种或多种，物质A为牛磺酸和/或磺胺。该功能性焦糖作为阻燃整理剂的应用过程是将功能性焦糖作为阻燃整理剂对纤维制品进行染整加工；所述纤维制品中的纤维为聚酰胺纤维。染整加工后的纤维制品的烟密度为5～12，且染整加工后的纤维制品的阻燃等级为V‑0级，且耐水洗。本发明中的功能性焦糖，用于聚酰胺织物的整理后，阻燃性能良好，符合V‑0级的标准，而且具有较强的耐水洗性能。

塞来昔布的有关物质及其制备方法和应用

本发明公开了塞来昔布的有关物质及其制备方法和应用，属于药物合成技术领域，解决了现有技术中尚未有对塞来昔布的N‑亚硝基化合物有关物质进行研究的问题。本发明的塞来昔布的有关物质结构如式I所示，本发明还公开了该有关物质的制备方法，及其在检测塞来昔布中间体、原料药和/或制剂中的应用。本发明首次提供了塞来昔布的N‑亚硝基化合物有关物质及制备方法，为塞来昔布的质量研究、标准研究、稳定性研究、药品不良反应的机制研究提供了基础；同时，为塞来昔布的生产、包装、储存、运输及应用条件的选择提供依据。

Solid phase fluorescence labeling reagents and uses thereof

A solid phase reagent and method for simultaneously capturing and fluorescently labeling an analyte with multiple reactive sites to provide a mono-labeled analyte are disclosed. The reagent can be used in the method and comprises a plurality of analyte-reactive groups tethered to a porous solid phase, wherein each analyte-reactive group is covalently attached to a fluorescent group either directly or indirectly, wherein the distance between adjacent analyte-reactive groups is greater than the gyration radius of a captured analyte; the fluorescent group is covalently attached to a cleavable anchor group either directly or through a first spacer; and the cleavable anchor group is covalently attached to the solid phase either directly or through a second spacer, wherein the solid phase is a porous solid or a porous gel.