p,p-methylene-bis-(benzene sulphonyl hydrazide)

The invention comprises p: p1-methylene-bis-(benzenesulphonyl hydrazide) of the formula It is prepared from diphenyl methane by treating with chlorosulphonic acid to give the disulphonyl chloride which is then treated with hydrazine. In an example the preparation of p: p1-methylene bis (benzenesulphonyl chloride) and p: p1-methylene bis (benzenesulphonyl hydrazide) by the above method is described.

Sulfonamide inhibitors of 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 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 aspartyl protease using the compounds of this invention and methods for screening compounds for anti-HIV activity.

Sulfonamide inhibitors of aspartyl protease

Sulfonamide inhibitors of aspartyl protease.

Sulfonamide inhibitors of aspartyl protease

Sulfonamide inhibitors of aspartyl protease

INDAN-1,3-DION AND INDAN-1,2,3-TRIONDERIVATE, PROCEDURE FOR YOUR PRODUCTION AND THEIR THERAPEUTIC USE

Hardnesses of gel

Procedure for the production of new Benzolsulfonylsemicarbaziden

SULFONE AMIDE DERIVATIVES

HYDRAZINE DERIVATIVES

Polynucleotide labelling reagent

Azaphenylalanine derivatives and their use as antithrombotic agents

BRANCHED CHAIN AMINO ACID-DEPENDENT AMINOTRANSFERASE INHIBITORS AND THEIR USE IN THE TREATMENT OF NEURODEGENERATIVE DISEASES

Imine derivates of madurahydroylacton, method for their production and pharmaceutical preparations containing these compounds

Sulfonylguanidine

SULFONYLHYDRAZINES AND THEIR USE AS ANTINEOPLASTIC AGENTS AND AS ANTITRYPANOSOMAL AGENTS

Sulfonylhydxazines of the formula RS02N(CH2CH2X)N(SO2CH3)2, wherein R is an alkyl or an aryl and X is a halogen or OSO2Y, wherin Y is an alkyl or an aryl. Such sulfonylhydrazines are useful in treating cancer. Methylating agents of the formula (a) R'SO2N(CH3)N(SO2CH3)2, wherein R' is an alkyl or an aryl and (b) R''SO2N(CH3)N(CH3)SO2R", wherein R'' is an alkyl or an aryl. Such methylating agents are useful as antitrypanosomal and anticancer agents.

Verfahren zur Herstellung neuer Benzolsulfonylsemicarbazide

Acrylic acid derivs for hardening photographic gelatine

Acrylic acid derivs. for hardening gelatine, esp. in the form of photographic emulsions, have the formula (I) (H2C=HC-OC-NH-OC-O)2-Y2 (II) (H2C=CH-OC-NH-OC-NH)2-Y3 (III) X and Z = O, S, NH, or NHCO bonded to Y through the C atom; Y = (CH2)m-, -CH2-CH2-(O-CH2-CH2) q-, -(CH2)r-O-(CH2)r-or -(CH2)r-S-(CH2)r-; or can be CO, or a direct bond when both X and Z are NH and N = 1; and m, n, r and q are positive integers, n is not > 2, m is not > 14, q = 2-4, and r = is not > 4. 0.5-5% wt. (I) is added opt. as a soln. in water, ethanol, dimethylformamide, etc. to the gelatine. The gelatine becomes hardened by the crosslinking action of (I). The use of cpds. (I) does not alter the photographic properties of the light sensitive gelatine layers.

Verfahren zur Herstellung farbkorrigierter farbenphotographischer Bilder

New azaphenylalanine derivatives are thrombine inhibitors useful to treat or inhibit thrombin, fibrin or thrombus formation in the blood

Azaphenylalanine derivatives (I) and their salts are new. Azaphenylalanine derivatives of formula (I) and their salts are new. [Image] R1>, Z : H, -C(=NR4>)NH2 or CH2-NH3+>Cl->; R4>H, 1-3C alkyl, OH, O-(1-3C alkyl) or NH2; R2>heterocyclic derivative of formula (1-3), azepine o r N(R8>)R9>; R5>-R7>H, 1-3C alkyl or COOR1>0>; R1>0>H or 1-3C alkyl; R8>, R9>H, 1-3C alkyl or 3-6C cycloalkyl; R1>1>H, 1-3C alkyl or benzyl; X : CH, O or S; Y : NR1>2>, O or S; R1>2>H, COCH3 or 1-3C alkyl; and R3>group of formula (4-6) or napthylsufonyl, benzylderivative of formula (9) (where R1> = -CH2-NH3+>Cl->). Provided that: (1) one of R1> and Z is H; and (2) R3>can only be napthylsulfonyl when R1> is -CH2>-NH3+>Cl-> An independent claim is also included for preparation of (I). ACTIVITY : Anticoagulant. MECHANISM OF ACTION : Thrombine inhibitor; Factor Xa inhibitor. (I) were tested for their thrombin inhibitory activity using enzyme assay. The negative logarithm of inhibitory constant for (4-{[1-{[Cyclopentyl ...

NEW HYDRAZIDE COMPOUNDS, A PROCESS FOR THEIR PREPARATION AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM

INHIBITORS OF GISTONATsETILTRANSFERAZ FAMILY MYST

NEW HYDRAZIDE COMPOUNDS, A PROCESS FOR THEIR PREPARATION AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM

НОВЫЕ ГИДРАЗИДНЫЕ СОЕДИНЕНИЯ, СПОСОБ ИХ ПОЛУЧЕНИЯ И СОДЕРЖАЩИЕ ИХ ФАРМАЦЕВТИЧЕСКИЕ КОМПОЗИЦИИ

... 1. Соединения формулы (I) R-NH-A-CO-NH-NH-(W)n-Z (I) где n равен 0 или 1, W обозначает группу -СО- или группу S(O)r, где r равен 0, 1 или 2, Z обозначает группу, выбранную из необязательно замещенного арила, необязательно замещенного арилалкила, необязательно замещенного гетероарила и необязательно замещенного гетероарилалкила, R обозначает группу, выбранную из: Z1-T-CO- Z1-O-T-CO- Z1-T-O-CO- Z1-T-S(O)q- где Z1 обозначает необязательно замещенную арильную, необязательно замещенную арилалкильную, необязательно замещенную гетероарильную или необязательно замещенную гетероарилалкильную группу, Т обозначает σ-связь или алкиленовую, алкениленовую или алкиниленовую группу, q обозначает целое число 0, 1 или 2, А обозначает линейную или разветвленную алкиленовую группу, имеющую 3-8 атомов углерода, линейную или разветвленную алкениленовую группу, имеющую 3-8 атомов углерода, линейную или разветвленную алкиниленовую группу, имеющую 3-8 атомов углерода, алкиленциклоалкиленовую группу, циклоалкиленалкиленовую ...

PROCESS FOR HARDENING GELATINE BY REACTING WITH ACRYLIC ACID DERIVATIVES

Process for the preparation of sulfohydrazides, additives in particular

Method for manufacturing organic sulfonyl semicarbazides

NOVEL METHOD OF SYNTHESIZING (E) STILBENE PERM FOR OBTAINING THE RESVERATROL THE PICEATANNOL AND

SULFONATED AMINO ACID DERIVATIVES AND METALLOPROTEINASE INHIBITORS CONTAINING THE SAME

하기 화학식 (I)로 표현되는, 메탈로프로테이나제 저해 활성을 갖는 화합물, 그의 광학적 활성 이성질체, 이들의 약제학적 수용가능염 또는 이들의 수화물. Claims 1. A compound having metalloproteinase inhibitory activity, represented by the following formula (I), an optically active isomer thereof, a pharmaceutically acceptable salt thereof or a hydrate thereof. [화학식 1] [Chemical Formula 1]

HYDRAZIDE COMPOUNDS, PROCESS FOR THEIR PREPARATION AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM

PURPOSE: Hydrazide compounds have a novel structure which imparts to them great affinity for NPY receptors. Accordingly, they are useful in treating pathologies associated with eating behavior disorders or energy-balanced disorders, such as diabetes, obesity, bulimia, anorexia nervosa, and arterial hypertension, anxiety, depression, epilepsy, and sexual dysfunction. CONSTITUTION: A compounds are represented by formula (I), wherein n is 0 or 1; W represents a -CO- group or an S(O)r group wherein r is 0, 1 or 2; Z represents a group selected from optionally substituted aryl, optionally substituted arylalkyl, optionally substituted heteroaryl and optionally substituted heteroarylalkyl; R represents a group selected from: Z1-T-CO-, Z1-O-T-CO-, Z1-T-O-CO-, Z1-T-S(O)q-, wherein Z1, T and q are as defined in the description; A represents an alkylene or alkylene group each having from 3 to 8 carbon atoms, an alkylenecycloalkylene, cycloalkylenealkylene or alkylenecycloalkylenealkylene, alkylenearylene ...

PESTICIDE 3- (SUBSTITUTED FENIL) - 5- (TIRNIL OR FURIL) - 1, 2, 4-TRIAZÓIS

THERAPEUTIC AMIDES AND RELATED COMPOUNDS

Disclosed herein is a compound having a structure: Therapeutic methods, compositions, and medicaments relating thereto are also disclosed.

POLYNUCLEOTIDE LABELLING REAGENT

The present invention provides a new labelling reagent for preparing modified oligonucleotides and processes for their production wherein these oligonucleotides contain at least υnce the structure P = N - SO2 - Benzole - L - M - X , characterized in that L is either - (CH2)n - or Polyethylenglycol, M is selected from a group consisting of - NH - , - O -, - S - ,. and - COO -, and X is either a protecting group or a detectable unit. L is preferably either - (CH2)n - or Polyethylenglycol.

LIPOIC ACID DERIVATIVES AND THEIR USE IN TREATMENT OF DISEASE

L'invention concerne l'identification d'une nouvelle classe d'agents thérapeutiques qui ciblent et détruisent de manière sélective les cellules tumorales et certains autres types de cellules malades, ainsi que des compositions comprenant des dérivés d'acide lipoïque attaquant spécifiquement le complexe pyruvate déshydrogénase dans ces cellules. L'invention concerne également des traitements contre le cancer et d'autres maladies, comprenant l'administration de quantités thérapeutiquement efficaces de dérivés d'acide lipoïque. Ces dérivés d'acide lipoïque présentent un large éventail d'applications thérapeutiques.

Optical switch systems using waveguide grating-based wavelength selective switch modules

The present invention discloses methods and apparatus for constructing optical switch systems, in which any input optical signals can be routed to any output ports. The methods and apparatus provide advantages of configuration flexibility, modular construction, constant signal loss, and minimal numbers of switch units required. The switch systems comprise MxN switch modules. The switch module in turn comprises a two-dimensional waveguide array and a number of waveguide grating-based wavelength selective switches. With the capability of wavelength-selective routing provided by the switch modules, the optical switch systems requires a relatively small amount of switch units to extend into a very-large-scale switch system.

Amidinophenylalanine derivatives as thrombin inhibitors

The compounds of the formula (formula 1) and pharmaceutically acceptable salts thereof and a process for preparing the same and pharmaceutical compositions containing the same are described wherein the substituents have the meaning as specified in the description. The compounds are used as thrombon inhibitors.

Sulfonated amino acid derivatives and metalloproteinase inhibitors containing the same

Compounds having a metalloproteinase inhibitory activity, represented by the formula (I), its optically active isomers, their pharmaceutically acceptable salts, or hydrates thereof.

Derivatives of indan-1,3-dione and indan-1,2,3-trione, methods of preparing them and therapeutic use thereof

PCT No. PCT/FR93/00329 Sec. 371 Date Mar. 24, 1994 Sec. 102(e) Date Mar. 24, 1994 PCT Filed Apr. 1, 1993 PCT Pub. No. WO93/20046 PCT Pub. Date Oct. 14, 1993Compounds of use in therapy and having the formula: (I) in which R2 and R3 independently denote H, C1-C4 alkoxy or OH and (A, B)=(oxygen, oxygen) in which case one out of R and R1 denotes OH, halogen, secondary amino or tertiary amine and the other denotes NHCOR4, NHNHCOR5 or NHNHCOCONH2, or R and R1 together form =N-NH-CO-R'5, =N-NH-CO-CO-NH2, (=N-NH-R6, =N-R7, =N-O-CO-R8 or =C(CH3)-NH-NH-CO-R9; or (A, B) =(N-NH-CX-NHR10, oxygen) in which case R and R1 together form =N-OH.

POLYMERIZABLE MONOMER, POLYMERIC COMPOUND, CHARGE CONTROL AGENT CONTAINING THE POLYMERIC COMPOUND, AND DEVELOPER BEARING MEMBER AND TONER WHICH CONTAIN THE CHARGE CONTROL AGENT

To provide a polymeric compound having superior charge-providing properties, the polymeric compound contains at least one unit represented by the following general formula (5). In the general formula (5), R1 represents a hydrogen atom or an alkyl group; R2 to R4 each represent a hydrogen atom, an alkyl group, an alkoxy group, a hydroxyl group or a halogen atom, or R3 and R4 may combine each other to form a ring; and A represents a divalent linking group.

Alpha-7 nicotinic acetylcholine receptor modulators and uses thereof-I

The present invention relates to chemical compounds of formula (I), with the substituents as described in the specification, useful in the positive modulation of the alpha 7 nicotinic acetylcholine receptor (α7 nAChR). The invention also relates to the use of these compounds in the treatment or prevention of a broad range of diseases in which the positive modulation of α7 nAChR is advantageous, including neurodegenerative and neuropsychiatric diseases and also neuropathic pain and inflammatory diseases.

PROCESS FOR PREPARING TRIAZOLE SUBSTITUTED AZAINDOLEOXOACETIC PIPERAZINE DERIVATIVES AND NOVEL SALT FORMS PRODUCED THEREIN

СПОСОБ ПРОИЗВОДСТВА ДЛИННОЦЕПОЧЕЧНОГО СПИРТА ЦИКЛОГЕКСЕНОНА ВЫСОКОЙ СТЕПЕНИ ОЧИСТКИ

Изобретение относится к способу получения длинноцепочечного спирта циклогексенона высокой чистоты, представленного формулой I, металлопосредованной межмолекулярной реакцией Барбье, опосредованной литием. Способ в соответствии с данным изобретением обладает преимуществом короткой схемы, высокого выхода и продукта высокой чистоты и подходит для промышленного применения. 5 н. и 3 з.п. ф-лы, 21 пр. РОССИЙСКАЯ ФЕДЕРАЦИЯ (19) RU (11) (13) 2 745 062 C2 (51) МПК C07C 49/753 (2006.01) C07C 45/64 (2006.01) C07C 49/713 (2006.01) C07C 45/65 (2006.01) C07C 281/12 (2006.01) C07C 311/49 (2006.01) ФЕДЕРАЛЬНАЯ СЛУЖБА C07C 303/40 (2006.01) ПО ИНТЕЛЛЕКТУАЛЬНОЙ СОБСТВЕННОСТИ C07D 309/12 (2006.01) (12) ОПИСАНИЕ ИЗОБРЕТЕНИЯ К ПАТЕНТУ (52) СПК C07C 49/753 (2021.01); C07C 45/64 (2021.01); C07C 49/713 (2021.01); C07C 45/65 (2021.01); C07C 281/12 (2021.01); C07C 311/49 (2021.01); C07C 303/40 (2021.01); C07D 309/12 (2021.01) (21)(22) Заявка: 2018131239, 03.02.2017 03.02.2017 Дата регистрации: Приоритет(ы): (30) Конвенционный приоритет: 03.02.2016 CN 201610077424.7 (43) Дата публикации заявки: 03.03.2020 Бюл. № 7 (45) Опубликовано: 18.03.2021 Бюл. № 8 (86) Заявка PCT: C 2 C 2 (85) Дата начала рассмотрения заявки PCT на национальной фазе: 03.09.2018 (56) Список документов, цитированных в отчете о поиске: Huber T. et al. Experimental Studies on the Selective beta-C-H Halogenation of Enones. The Journal of Organic Chemistry, 2015, Vol.80, No.4, P. 2281-2294. Murugan R. Solvent Free Rapid Synthesis of 3-Alkoxycyclohex-2-en1-one from 1,3-Cyclohexanedione Promoted by Indium(III) Chloride/Silica Gel. Australian Journal of Chemistry, 2005, Vol.58, (см. прод.) CN 2017/072855 (03.02.2017) (87) Публикация заявки PCT: 2 7 4 5 0 6 2 WO 2017/133675 (10.08.2017) R U 2 7 4 5 0 6 2 (73) Патентообладатель(и): ТАЙХО ФАРМАСЬЮТИКАЛ КО., ЛТД. (JP) 18.03.2021 R U (24) Дата начала отсчета срока действия патента: (72) Автор(ы): ЦЗЯН, Дехуэй (CN), ШЭНЬ, Сяоцзюнь (CN), ЧЖАН, Цзянь (CN) Адрес для переписки: 129090, ...

ФЕНИЛГИДРАЗИНОВЫЕ ПРОИЗВОДНЫЕ, СПОСОБ БОРЬБЫ С ВРЕДИТЕЛЯМИ И ИНСЕКТОАКАРИЦИДОНЕМАТОЦИДНАЯ КОМПОЗИЦИЯ

Изобретение относится к соединениям, имеющим структурную формулу I, где X, Y, R и Z определены в описании заявки. Соединения по изобретению являются эффективными в борьбе против клещей, нематод, цикадки рисовой, совки и блошки длинноусой. Описаны также способы получения указанных соединений. Структурная формула I где - простая или двойная связь. 3 с. и 11 з.п.ф-лы, 8 табл.

ДИЗАМЕЩЕННЫЕ ФУРАНОНЫ, ТИАЗОЛЫ И ПЕНТЕНОНЫ В КАЧЕСТВЕ ИНГИБИТОРОВ ЦИКЛООКСИГЕНАЗЫ, СПОСОБ ИХ ПОЛУЧЕНИЯ, ФАРМАЦЕВТИЧЕСКАЯ КОМПОЗИЦИЯ И СПОСОБ ЛЕЧЕНИЯ

Описывается соединение формулы 1 или его фармацевтически приемлемая соль, где X-Y-Z выбирают из группы, включающей в себя a) -C(O)CH2CH2-, b) -С(O)-O-CR5(R5)-, c) -S-N= CH, d) -CH=N-S-, когда сторона b) представляет собой двойную связь, а сторона a) и c) представляют собой простые связи; и X-Y-Z представляет группу =N-S-CH=, когда стороны a и c представляют собой двойные связи, а сторона b представляет собой простую связь; R1 выбирают из группы, включающей в себя a) S(O)2CH3, b) S(O)2NH2, c) S(O)2NHC(O)CF3; R2 выбирают из группы, включающей в себя a) C3, C4, C5, C6 и C7-циклоалкил, b) моно-, ди- или тризамещенный фенил, в котором заместители выбирают из группы, включающей в себя (1) водород, (2) галоген, (3) C1-6-алкокси, (4) C1-6-алкилтио, (5) -CO2H; R5 и R6 каждый независимо выбарают из группы, включающей в себя (a) водород, (b) C1-6-алкил. Описывается также способ получения вышеуказанных соединений, способ лечения и фармацевтическая композиция на основе соединений формулы 1 для лечения ...

НОВЫЙ СПОСОБ СИНТЕЗА (Е)-СТИЛЬБЕНОВЫХ ПРОИЗВОДНЫХ, КОТОРЫЙ ПОЗВОЛЯЕТ ПОЛУЧИТЬ РЕСВЕРАТРОЛ И ПИСАТАННОЛ

... 1. Способ синтеза (Е)-стильбенового производного формулы (VI) ! ! в которой ! А представляет собой водород или группу OR2, и ! R1, R2, R'1 и R'2 представляют собой, независимо друг от друга, линейную или разветвленную алкильную группу, содержащую от 1 до 6 атомов углерода, или аралкильную группу, содержащую от 7 до 16 атомов углерода, которая необязательно замещена одной или несколькими алкокси- или галогеновыми группами, причем для R1 и R2 также возможно образование углеводородной цепи -(СН2)n- c n=1-3, отличающийся тем, что соединение формулы (III) ! ! в которой А, R1, R2, R'1 и R'2 имеют значения, определенные выше, R представляет собой линейную или разветвленную алкильную группу, содержащую от 1 до 6 атомов углерода, ! подвергают взаимодействию в качестве промежуточного соединения, ! из которого декарбоксилированием получают соединение формулы (IV) ! ! в которой А, R1, R2, R'1 и R'2 имеют значения, определенные выше, затем соединение формулы (IV) ! либо восстанавливают в спирт, тогда ...

Verfahren zur Herstellung von Benzolsulfonyl-semicarbaziden

Preparation of sulfonyl semicarbozides

Organic sulphonyl semicarbazides are prepared by reacting the corresponding organic sulphanhydrazide with urea in solution in an aqueous acidic reaction medium. Preferred products include RSO2NHNHCONH2, R1(SO2NHNHCONH2)n and X(C6H4SO2NHNHCONH2)2 where R and R1 are aliphatic, cycloaliphatic, araliphatic or aromatic hydrocarbon radicals which are optionally further substituted, n is 1, 2 or 3 and X represents oxygen, sulphur, sulphonyl, sulphoxide or methylene.

INDAN-1,3-DION AND INDAN-1,2,3-TRIONDERIVATE, PROCEDURE FOR YOUR PRODUCTION AND YOUR THERAPEUTIC USE

HEMMER THE BRANCH OUT-AMINO ACID-DEPENDENT AMINOTRANSFERASE AND THEIR USE IN THE TREATMENT OF NEURODEGENERATIVE ILLNESSES

DERIVATIVES OF PHENYL (THIO) UREA AND PHENYL (THIO) CARBAMAT FUNGICIDES

PROCEDURE FOR THE PRODUCTION OF TRIAZOLSUBSTITUIERTEN AZAINDOLOXOESSIGSÄUREPIPERAZINDERIVATEN AND MANUFACTURE NEW SALZFORMEN

SALTS OF LIPONSAÜREDERIVATEN AND THEIR USE WITH THE TREATMENT OF DISEASES

HYDRAZINE DERIVATIVES

Procedures for the production of new Benzolsulfonyl semicarbaziden

Procedure for the production more again Benzolsulfonyl semicarbazide

Procedure for the production of new Benzolsulfonylsemicarbaziden

Glucagon antagonists/inverse agonists

AZAPHENYLALANINE DERIVATIVES AND THEIR USE AS ANTITHROMBOTIC AGENTS

Substituted hydrazinophenylsulfonyl ureas, a process for preparing the same and their use as herbicides and plant growth regulators

Alpha7 nicotinic acetylcholine receptor modulators and uses thereof-i

The present invention relates to chemical compounds of formula (I), with the substituents as described in the specification, useful in the positive modulation of the alpha 7 nicotinic acetylcholine receptor (7 nAChR). The invention also relates to the use of these compounds in the treatment or prevention of a broad range of diseases in which the positive modulation of 7 nAChR is advantageous, including neurodegenerative and neuropsychiatric diseases and also neuropathic pain and inflammatory diseases.

HYDRAZINE DERIVATIVES

Hydrazine derivatives of formula (I) wherein R1 represents lower alkyl, lower alkenyl, lower cycloalkyl, lower cycloalkyl-lower alkyl, aryl or aryl-lower alkyl, R2 represents heterocyclyl or NR5R6, R3 represents hydrogen, lower alkyl, halo-lower alkyl, cyano-lower alkyl, hydroxy-lower alkyl, amino-lower alkyl, lower alkoxy-lower alkyl, lower alkoxycarbonyl-lower alkyl, lower cycloalkyl-lower alkyl, aryl-lower alkyl, heterocyclyl-lower alkyl, heterocyclylcarbonyl-lower alkyl, lower alkenyl, lower alkynyl, lower cycloalkyl, aryl, heteroaryl or aryl-lower alkyl, R4 represents lower alkyl, lower alkenyl, lower cycloalkyl-lower alkyl or a grouping of the formula-Z- aryl, -Z-heterocyclyl or-(CH2)n-CH=CR7R8, R5 and R6 each independently represent hydrogen or lower alkyl, R7 and R8 each independently represent hydrogen or lower alkyl or R7 and R8 together represent lower alkylene in which one CH2 group is optionally replaced by a hetero atom, X and Z each represent a spacer group, and n stands ...

N, N'-BIS(SULFONYL) HYDRAZINES HAVING ANTINEOPLASTIC ACTIVTY

Compounds of the formula where R is methyl or 2-chloroethyl, and R1 and R2 are each an aromatic hydrocarbon, ring substituted aromatic hydrocarbon moiety, or an alkyl moiety. The compounds have been found to be alkylating agents having antineoplastic activity.

PHENYL HETEROCYCLES AS COX-2 INHIBITORS

The invention encompasses the novel compound of Formula (I) useful in the treatment of cyclooxygenase-2 mediated diseases. The invention also encompasses certain pharmaceutical compositions for treatment of cyclooxygenase-2 mediated diseases comprising compounds of Formula (I).

PHENYL HETEROCYCLES AS CYCLOOXYGENASE-2 INHIBITORS

Compounds useful in the treatment of cyclooxygenase-2 mediated diseases are provided of formula (I): (see fig. I) wherein R1 is selected from the group consisting of (a) S(O)2CH3, and (b) S(O)2NH2, and R2 is unsubstituted, mono or di- substituted phenyl wherein the substituents are selected from the group consisting of halo, methoxy, methyl, said halo being selected from the group consisting of fluoro, chloro and bromo.

NOVEL TRIENOIC RETINOID COMPOUNDS AND METHODS

Novel trienoic retinoid compounds having activity for retinoic acid receptors and retinoid X receptors are provided. Also provided are pharmaceutical compositions incorporating such compounds and methods for their use.

INHIBITORS OF IDO

Phenyl heterocyclic compound used as epoxy enzyme-2 inhibitor

本发明公开了式A化合物，其中R 1 选自：(a)S(O) 2 CH 3 ，(b)S(O) 2 NH 2 ，R 2 选自一或二取代的苯基，其中取代基选自：(1)氢，(2)卤素，(3)C 1-4 烷氧基，(4)C 1-4 烷硫基，(5)CN，(6)CF 3 ，(7)C 1-4 烷基，(8)N 3 ，和(9)-C(R 5 )(R 6 )-OH；R 5 和R 6 各自独立地选自：(a)氢，(b)甲基或乙基，或R 5 和R 6 与它们所连的碳原子一起形成4、5或6个原子的饱和碳环。

DERIVED FROM PHENYL (THIO) UREAS AND PHENYL (THIO) FUNGICIDAL CARBAMATES

L'invention concerne des composés de formule (I) ainsi que leurs sels, possédant des activités fongicides : (CF DESSIN DANS BOPI) dans laquelle les divers radicaux et substituants sont tels que définis dans la description,ainsi que les compositions fongicides qui les contiennent et les méthodes de luttes contre les champignons phytopathogènes des cultures à l'aide de ces composés et compositions. The invention relates to compounds of formula (I) as well as their salts, having fungicidal activities: (DRAWING IN BOPI) in which the various radicals and substituents are as defined in the description, as well as the fungicidal compositions which contain them and methods of controlling phytopathogenic fungi of crops using these compounds and compositions.

Method for producing bis(sulfonyl)imide ammonium salts, bis(sulfonyl)imide, and bis(sulfonyl)imide lithium salts

Provided is a method for producing bis(sulfonyl)imide ammonium salts, bis(sulfonyl)imide, and bis(sulfonyl)imide lithium salts in a simple manner and with good yield. A method for producing bis(sulfonyl)imide ammonium salts, wherein ammonia is reacted in the absence of a catalyst with a compound represented by the general formula of R-CHF-SO2X (wherein R is a fluorine atom or fluorine-containing alkyl group which may include a C1-C4 ethereal oxygen atom, and X is fluorine or chlorine). Furthermore, a method for producing bis(sulfonyl)imide and bis(sulfonyl)imide lithium salts, wherein the bis(sulfonyl)imide ammonium salts are employed.

SOLUBLE DIAZOALKANE PRECURSORS

The present invention relates to compounds useful in the preparation of diazoalkanes in general (such as diazomethane, diazoethane, diazopropane, diazobutane and homologues) and to diazomethane (CH2=N=N) in particular. The compounds chosen as the diazomethane source according to the invention also have the advantage of being water soluble. They are capable of being decomposed to diazomethane or another diazoalkane (which is allowed to bubble out of the vessel to another vessel containing a solution of reactant) and are converted to by-products that are also water-soluble.

INDAN-1,3-DIONE AND INDAN-1,2,3-TRIONE DERIVATIVES, PROCESSES FOR PREPARATION OF SAME AND THEIR USE AS THERAPEUTIC AGENTS

Compounds of formula (I) used as therapeutic agents in which R2 and R3 are independently H, C1-C4 alkoxy or OH and (A, B) = (oxygen, oxygen) in which case either R or R1 is OH, halogen, secondary amino or tertiary amine while the other denotes NHCOR4, NHNHCOR5 or NHNHCOCONH2 or R and R1 together form =N-NH-CO-R'5, =N-NH-CO-CO-NH2, =N-NH-R6, =N-R7, =N-O-CO-R8 or =C(CH3)-NH-NH-CO-R9; or (A,B) = (N-NH-CX-NHR10, oxygen) in which case R and R1 together form =N-OH.

2,6-DIHALOBENZALDEHYDE SULFONYL HYDRAZONES

AMIDINOPHENYLALANINE DERIVATIVES AS THROMBIN INHIBITORS

СПОСОБ ПРОИЗВОДСТВА ДЛИННОЦЕПОЧЕЧНОГО СПИРТА ЦИКЛОГЕКСЕНОНА ВЫСОКОЙ СТЕПЕНИ ОЧИСТКИ

FIELD: chemical or physical processes.SUBSTANCE: present invention relates to a method of producing a long-chain cyclohexenone alcohol represented by formula I, where A is Calkylene, R, Rand Rare each independently methyl, and the method includes the following steps: (1a) a condensation reaction of a crude product of a long-chain cyclohexenone III and hydrazine or derivative thereof RNHNH, where Risor, Ris 4-methylphenyl or amino, to obtain compound II, and (1b) hydrolysis of compound II in the presence of an acidic substance to obtain compound I.Invention also relates to intermediate compounds and use thereof for producing a compound of formula I.EFFECT: present invention enables to obtain alcohol of formula I of high degree of purity.22 cl, 2 tbl, 32 ex РОССИЙСКАЯ ФЕДЕРАЦИЯ (19) RU (11) (13) 2 729 186 C2 (51) МПК C07C 45/42 (2006.01) C07C 249/16 (2006.01) C07C 49/713 (2006.01) C07C 49/753 (2006.01) C07C 251/84 (2006.01) C07C 311/49 (2006.01) ФЕДЕРАЛЬНАЯ СЛУЖБА ПО ИНТЕЛЛЕКТУАЛЬНОЙ СОБСТВЕННОСТИ (12) ОПИСАНИЕ ИЗОБРЕТЕНИЯ К ПАТЕНТУ (52) СПК C07C 45/42 (2020.02); C07C 249/16 (2020.02); C07C 49/713 (2020.02); C07C 49/753 (2020.02); C07C 251/84 (2020.02); C07C 311/49 (2020.02) (21)(22) Заявка: 2018130292, 22.01.2017 22.01.2017 Дата регистрации: Приоритет(ы): (30) Конвенционный приоритет: 22.01.2016 CN 201610044990.8 (43) Дата публикации заявки: 25.02.2020 Бюл. № 6 (45) Опубликовано: 05.08.2020 Бюл. № 22 (86) Заявка PCT: CN 2017/072078 (22.01.2017) C 2 C 2 (85) Дата начала рассмотрения заявки PCT на национальной фазе: 22.08.2018 (56) Список документов, цитированных в отчете о поиске: WO 2004/087630 A1, 14.10.2004. WO 2000047199 A1, 17.08.2000. Ferhad Shirini et al. Efficient oxidative cleavage of C=N using chromium trioxide supported on NaHSO4⋅H2O. Arkivoc, 2007, 1, 34-39. RU 2100346 C1, 27.12.1997. (87) Публикация заявки PCT: 2 7 2 9 1 8 6 WO 2017/125087 (27.07.2017) R U 2 7 2 9 1 8 6 (73) Патентообладатель(и): ТАЙХО ФАРМАСЬЮТИКАЛ КО., ЛТД. (JP) 05.08.2020 R U (24) Дата ...

СПОСОБ ПРОИЗВОДСТВА ДЛИННОЦЕПОЧЕЧНОГО СПИРТА ЦИКЛОГЕКСЕНОНА ВЫСОКОЙ СТЕПЕНИ ОЧИСТКИ

РОССИЙСКАЯ ФЕДЕРАЦИЯ (19) RU (11) (13) 2018 131 239 A (51) МПК C07C 49/753 (2006.01) ФЕДЕРАЛЬНАЯ СЛУЖБА ПО ИНТЕЛЛЕКТУАЛЬНОЙ СОБСТВЕННОСТИ (12) ЗАЯВКА НА ИЗОБРЕТЕНИЕ (21)(22) Заявка: 2018131239, 03.02.2017 (71) Заявитель(и): ТАЙХО ФАРМАСЬЮТИКАЛ КО., ЛТД. (JP) Приоритет(ы): (30) Конвенционный приоритет: 03.02.2016 CN 201610077424.7 (85) Дата начала рассмотрения заявки PCT на национальной фазе: 03.09.2018 R U (43) Дата публикации заявки: 03.03.2020 Бюл. № 7 (72) Автор(ы): ЦЗЯН, Дехуэй (CN), ШЭНЬ, Сяоцзюнь (CN), ЧЖАН, Цзянь (CN) (86) Заявка PCT: (87) Публикация заявки PCT: WO 2017/133675 (10.08.2017) A Адрес для переписки: 129090, Москва, ул. Б. Спасская, 25, стр. 3, ООО "Юридическая фирма Городисский и Партнеры" R U (57) Формула изобретения 1. Способ получения длинноцепочечного спирта циклогексенона высокой чистоты, представленного формулой I, по следующей схеме реакции: где A является C10-18алкиленом, R1, R2 и R3 каждый независимо является H или метилом, и R4 является H, замещенным или незамещенным C1-7алкилом, замещенным или незамещенным C6-14арилом, или , где замещенный означает замещенный одним заместителем или двумя или более заместителями, выбранными из метила, нитро, хлора и брома; R5 является H, метокси, Стр.: 1 A 2 0 1 8 1 3 1 2 3 9 (54) СПОСОБ ПРОИЗВОДСТВА ДЛИННОЦЕПОЧЕЧНОГО СПИРТА ЦИКЛОГЕКСЕНОНА ВЫСОКОЙ СТЕПЕНИ ОЧИСТКИ 2 0 1 8 1 3 1 2 3 9 CN 2017/072855 (03.02.2017) трет-бутокси, бензилокси, фенилом, 4-метилфениломили амино; и R4 предпочтительно является или , где способ включает стадии (1a) реакцию конденсации неочищенного продукта длинноцепочечного спирта циклогексенона III и гидразина или его производного R4NHNH2 с получением соединения II, и (1b) гидролиз соединения II в присутствии кислого вещества с получением соединения I высокой чистоты, где неочищенный продукт длинноцепочечного спирта циклогексенона III получают по следующей схеме реакции: A 2 0 1 8 1 3 1 2 3 9 R U A Стр.: 2 2 0 1 8 1 3 1 2 3 9 где A является C10-18алкиленом и X является галогеном. ...

ФТОРАЛЛИЛСУЛЬФОНИЛАЗИДНЫЕ МОНОМЕРЫ И ПОЛУЧЕННЫЕ ИЗ НИХ ПОЛИМЕРЫ

1. Сульфонилазидаллильный мономер формулы: CF=CF-CF-O-R-SON, формула (I), где Rобозначает двухвалентную (пер)фторированную группу, необязательно, содержащую один или более атомов кислорода эфирной группы [мономер (Az)].2. Мономер (Az) по п. 1, где указанный мономер соответствует формуле (Ia): CF=CF-CF-O-CF-R'-SON, формула (Ia), где R' обозначает двухвалентную C-C(пер)фторированную группу, необязательно, содержащую один или атомов кислорода эфирной группы.3. Мономер (Az) по п. 2, где указанный мономер соответствует приведенной здесь ниже формуле (Ib): CF=CF-CF-O-CF-CF-SON, формула (Ib).4. Способ получения мономера (Az) по любому из пп. 1-3, включающий взаимодействие фторсульфонового предшественника формулы (II): CF=CF-CF-O-R-SOF, формула (II), где Rобозначает двухвалентную (пер)фторированную группу, необязательно, содержащую один или более атомов кислорода эфирной группы, с азидной солью [соль (Az)].5. Фторполимер [полимер (F)], содержащий повторяющиеся единицы, получаемые, по меньшей мере, из одного мономера (Az), который определен в любом из пп. 1-3, и необязательно повторяющиеся единицы, получаемые, по меньшей мере, из одного этилен-ненасыщенного фторированного мономера [мономер (F)], отличного от мономера (Az), и/или повторяющиеся единицы, получаемые из этилен-ненасыщенного нефторированного мономера [мономер (H)].6. Полимер (F) по п. 5, где указанный полимер (F) содержит повторяющиеся единицы, получаемые, по меньшей мере, из одного мономера (Az), и повторяющиеся единицы, получаемые из винилиденфторида (VDF).7. Полимер (F) по п. 5, где указанный полимер (F) содержит повторяющиеся единицы, получаемые из винилиденфторида (VDF) и от 10 до 50 мол.%, предпочтительно от 15 до 40 мол.% повторяющихся единиц, получаемых из трифторэтилена (TrFE).8. Способ получения полимера (F) по любому из пп. 5-7, включающий полимеризацию в присутствии инициатора радика РОССИЙСКАЯ ФЕДЕРАЦИЯ (19) RU (11) (13) 2014 129 012 A (51) МПК C08F 14/18 (2006.01) ФЕДЕРАЛЬНАЯ СЛУЖБА ПО ...

HEMMER DER VERZWEIGTEN AMINOSÄURE-ABHÄNGIGEN AMINOTRANSFERASE UND DEREN VERWENDUNG IN DER BEHANDLUNG VON NEURODEGENERATIVEN ERKRANKUNGEN

ORGANISCHE HYDRAZIN-VERBINDUNGEN FUER PHARMAZEUTISCHE ANWENDUNG.

Azaphenylalaninderivate

Verbindung der Formel (I) wobei R1 und Z H sind oder ein Rest mit der Formel unter der Voraussetzung, dass eines von R1 und Z H ist; R4 = H, Alkyl (C1-C3), OH; o-Alkyl (C1-C3), NH2; R2 einen Rest der Formel darstellt wobei R5 = H, ALkyl (C1-C3), COOR10; R6 = H, Alkyl (C1-C3), C00R10; R7 = H, Alkyl (C1-C3), C00R10; R10 = H, Alkyl (C1-C3) R8 = H, Alkyl (C1-C3), Cycloalkyl (C3-C6) R9 = H, Alkyl (C1-C3) , Cycloalkyl (C3-C6) R11 = H, Alkyl (C1-C3), Benzyl, X = CH, O, S, Y = NR12, O, S, R12 = H, COCH3, Alkyl (C1-C3); R3 ist ein Rest der Formel oder ein Rest der Formel in dem Fall von R1 = und pharmazeutisch akzeptable Salze davon.

Hydroxylammonium and aloxylammonium compounds and their use as ionic liquids

An ionic liquid containing cations of the formula R<1>R<2>R<3>N<+>OR<4> and an anion wherein R<1>, R<2>, R<3> and R<4> are each independently selected from hydrogen and hydrocarbyl, the ionic liquid containing 1 % or less of water by mass. Preferably. R<1>, R<2>, R<3> are independently hydrogen, methyl, ethyl or 2-hydroxyethyl and R<4> is H. The preferred anions are bis(trifluoromethylsulphonyl)imide, glycolate and acetate. Such ionic liquids may be used in particular as solvents for biocatalysis, such as the chymotrypsin-catalysed transesterification of 1-propanol and D-phenylalanine acetyl ester. The OR<4> functionality is not readily esterifiable and is therefore stable for use in biocatalytic reactions involving hydrolases and similarly reactive moieties.

Aminosulfonylbensoates

Compounds of the general formula (wherein X and Y independently of each other are fluorine, chlorine, bromine or hydrogen, and R denotes alkyl, alkenyl, cycloalkyl, or benzyl) are antiviral agents.

p,p-oxybis (benzene sulfonyl hydrazide)

The invention comprises p,p1-oxybis (benzene sulphonyl hydrazide) and a method for preparing this compound by reacting p,p1-oxybis (benzene sulphonyl chloride) with hydrazine in the presence of ethyl alcohol. The reaction may also be carried out without a reaction solvent, or in the presence of water, methyl alcohol or dioxan in place of ethyl alcohol. A hydrogen chloride acceptor may be used in the reaction, e.g. an excess of hydrazine. One example is given. Specification 686,814 is referred to. p,p1-Bis (benzene sulphonyl hydrazide is prepared by the reaction of hydrazine and the corresponding sulphonyl chloride. p,p1-Oxybis (benzene sulphonyl chloride) is prepared by reacting diphenyl ether and chlorosulphonic acid. p,p1-Bis (benzene sulphonyl chloride) is prepared by reacting diphenyl ether with chlorosulphonic acid, and xenylene-2,21-sulphone-4,41-disulphonyl chloride and diphenyl monosulphonyl chloride are also formed. Methane- and benzene-sulphonyl hydrazide and naphthalene-2,7-disulphonyl ...

1-ALKYL-2-ACYL-1,2-DISULFONYLHYDRAZINE WITH ANTINEOPLASTI ACTIVITY

SULPHONYL HYDRAZINE AND THEIR USE AS ANTI-EOP READING TABLES AND AS ANTITRYPANOSOMALE MEANS.

LIPONSAÜREDERIVATE AND THEIR USE WITH THE TREATMENT OF DISEASES

THERAPEUTIC AMIDES AND APPROPRIATE CONNECTIONS

AZAPHENYLALANINE DERIVATIVES

ORGANIC HYDRAZINE CONNECTIONS FOR PHARMACEUTICAL APPLICATION.

PHENOXYPHENYLSULPHONYL COMPOUNDS

Phenyl heterocycles as cyclooxygenase-2 inhibitors

Sulfonated amino acid derivatives and metalloproteinase inhibitors containing the same

Bisubstituted carbocyclic cyclophilin binding compounds and theirus

SULFONAMIDE INHIBITORS OF 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 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 aspartyl protease using the compounds of this invention and methods for screening compounds for anti-HIV activity.

THERAPEUTIC AMIDES AND RELATED COMPOUNDS

Disclosed herein is a compound having a structure: Therapeutic methods, c ompositions, and medicaments relating thereto are also disclosed.

Methods for producing bis(sulfonyl)imide ammonium salt, bis(sulfonyl)imide and bis(sulfonyl)imide lithium salt

To provide methods for producing a bis(sulfonyl)imide ammonium salt, a bis(sulfonyl)imide and a bis(sulfonyl)imide lithium salt simply and in good yield. A method for producing a bis(sulfonyl)imide ammonium salt, which comprises reacting a compound of the formula R—CHF—SO 2 X (wherein R is a C 1-4 fluorinated alkyl group which may contain an etheric oxygen atom, or a fluorine atom, and X is a fluorine atom or a chlorine atom) with ammonia in the absence of a catalyst. Further, methods for producing a bis(sulfonyl)imide and a bis(sulfonyl)imide lithium salt by using the bis(sulfonyl)imide ammonium salt.

Phenolic hydrazone macrophage migration inhibitory factor inhibitors

Provided are various compounds of Formula (I): Also provided are pharmaceutical compositions comprising the above compounds. Additionally, methods of inhibiting macrophage migration inhibitory factor (MIF) activity in a mammal are provided, as are methods of treating or preventing inflammation in a mammal. Further provided are methods of treating a mammal having sepsis, septicemia, and/or endotoxic shock. Also provided are methods of treating a mammal having an autoimmune disease, and methods of treating a mammal having a tumor.

Stem cell differentiating agents and uses therefor

The present invention relates to screens for compounds that can induce stem cell differentiation. In addition, isoxazoles and sulfonyl hydrazones are identified as general classes of compounds that can induce differentiation of stem cells into cells of neuronal and cardiac fate, respectively.

Sulfonyl semicarbazides, semicarbazides and ureas, pharmaceutical compositions thereof, and methods for treating hemorrhagic fever viruses, including infections associated with arena viruses

Compounds, methods and pharmaceutical compositions for treating viral infections, by administering certain novel sulfonyl semicarbazides, carbonyl semicarbazides, semicarbazides, ureas and related compounds in therapeutically effective amounts are disclosed. Methods for preparing the compounds and methods of using the compounds and pharmaceutical compositions thereof are also disclosed. In particular, the treatment and prophylaxis of viral infections such as caused by hemorrhagic fever viruses is disclosed, i.e., including but not limited to, Arenaviridae (Junin, Machupo, Guanarito, Sabia, Lassa, Tacaribe, Pinchinde, and VSV), Filoviridae (ebola and Marburg viruses), Flaviviridae (yellow fever, omsk hemorrhagic fever and Kyasanur Forest disease viruses), and Bunyaviridae (Rift Valley fever).

PLASMINOGEN ACTIVATOR INHIBITOR-1 INHIBITORS AND METHODS OF USE THEREOF TO MODULATE LIPID METABOLISM

The invention relates to plasminogen activator-1 (PAI-1) inhibitor compounds and uses thereof in the treatment of any disease or condition associated with elevated PAI-1. The invention includes, but is not limited to, the use of such compounds to modulate lipid metabolism and treat conditions associated with elevated PAI-1, cholesterol, or lipid levels. 139.-. (canceled)44. A method of increasing circulating high density lipoprotein (HDL) in a subject claim 40 , comprising administering to said subject a plasminogen activator inhibitor-1 (PAI-1) inhibitor compound according to in an amount effective to increase HDL.45. A method of decreasing circulating very low density lipoprotein (VLDL) in a subject claim 40 , comprising administering to said subject a plasminogen activator inhibitor-1 (PAI-1) inhibitor compound according to in an amount effective to decrease VLDL.46. The method of claim 44 , wherein the subject is human.47. The method of claim 44 , wherein the PAI-1 inhibitor decreases PAI-1 binding to apolipoprotein E (ApoE) claim 44 , apolipoprotein A (ApoA) claim 44 , and/or VLDL.48. (canceled)49. (canceled)50. The method of claim 44 , wherein the PAI-1 inhibitor binds to PAI-1 in the presence of vitronectin.51. The method of claim 44 , wherein the PAI-1 inhibitor binds to PAI-1 in the presence of urokinase type plasminogen activator (uPA).52. A method of modulating cholesterol and/or lipid uptake comprising the step of administering a PAI-1 inhibitor compound according to in an amount effective to modulate cholesterol and/or lipid uptake.53. A method of modulating cholesterol and/or lipid clearance comprising the step of administering a plasminogen activator inhibitor-1 (PAI-1) inhibitor compound according to in an amount effective to inhibit very low density lipoprotein (VLDL) or apolipoprotein E (ApoE) or apolipoprotein A (ApoA) binding to VLDL-R and modulate cholesterol and/or lipid clearance.54. A method of modulating cholesterol and/or lipid clearance ...

SULFONYL HYDRAZIDE COMPOUNDS AND A REGIO-SELECTIVE PROCESS TO PREPARE 4-AROYL PYRAZOLE DERIVATIVES

Disclosed are compounds of Formula I, including all stereoisomers, (N-oxides), and salts thereof, wherein A and R are as defined in the disclosure. 2. The compound of wherein{'sub': 1', '4', '3', '7', '2', '4', '2', '4', '1', '4', '1', '4', '1', '4', '1', '4, 'A is phenyl, naphthalenyl, or a 5- or 6-membered heterocyclic ring, each ring or ring system optionally substituted with halogen, C-Calkyl, C-Ccycloalkyl, C-Calkenyl, C-Calkynyl, C-Calkoxy, C-Chaloalkyl, C-Chaloalkoxy or C-Chaloalkylthio; and'}{'sub': 1', '8', '1', '4', '1', '4', '2', '4', '2', '4', '1', '4', '1', '4', '1', '4, 'R is C-Calkyl optionally substituted with halogen or C-Calkoxy; or phenyl, naphthalenyl or a 5- or 6-membered heterocyclic ring, each ring or ring system optionally substituted with halogen, C-Calkyl, C-Calkenyl, C-Calkynyl, C-Calkoxy, C-Chaloalkyl or C-Chaloalkoxy.'}3. The compound of whereinA is phenyl, naphthalenyl, or a 5- or 6-membered heterocyclic ring, each ring or ring system optionally substituted with halogen; and{'sub': 1', '8', '1', '4', '1', '4', '1', '4, 'R is C-Calkyl optionally substituted with halogen or C-Calkoxy; or phenyl, naphthalenyl or a 5- or 6-membered heterocyclic ring, each ring or ring system optionally substituted with halogen, C-Calkyl or C-Calkoxy.'}4. The compound of wherein{'sub': 1', '4', '3', '7', '2', '4', '2', '4', '1', '4', '1', '4', '1', '4', '1', '4', '2', '4', '1', '4, 'A is phenyl, optionally substituted with halogen, C-Calkyl, C-Ccycloalkyl, C-Calkenyl, C-Calkynyl, C-Calkoxy, C-Chaloalkyl, C-Chaloalkoxy, C-Chaloalkylthio, C-Cdialkylamino, cyano, nitro, C-Calkoxycarbonyl, phenyl or phenoxy; and'}{'sub': 1', '8, 'R is C-Calkyl.'}5. The compound of whereinA is phenyl optionally substituted with halogen; and{'sub': '3', 'R is CH.'}6. The compound of whereinA is phenyl substituted with halogen at 3- and 5-positions or 2- and 5-positions; and{'sub': 1', '4, 'R is phenyl optionally substituted with C-Calkyl.'}7. The compound of wherein{'sub': 1', '4, ...

CRYOPYRIN INHIBITORS FOR PREVENTING AND TREATING INFLAMMATION

Inhibitors that are anti-inflammatory agents are provided, as are methods of using the analogs to inhibit inflammation and prevent or treat diseases and conditions associated with inflammation, such as heart failure and autoimmune diseases. 9. The method of claim 6 , wherein said NRLP3 inflammasome-associated inflammation is selected from the group consisting of adverse cardiac remodeling after acute myocardial infarction (AMI); peritonitis claim 6 , and an autoinflammatory condition. 1. Field of the InventionThe invention generally relates to improved anti-inflammatory agents and methods of their use to inhibit inflammation. In particular, the invention provides compounds that inhibit cryopyrin (NRLP3 or NALP3) inflammasome formation and activation, and methods of using the analogs to prevent or treat NRLP3 inflammasome associated diseases and conditions, such as heart failure and acute and chronic inflammatory diseases.2. Background of the InventionInflammasomes are protein complexes that recognize a diverse set of inflammation-inducing stimuli and control the production of important pro-inflammatory cytokines such as IL-1β and IL-18 through the activation of caspase-1. All inflammasomes share a similar structure and are typically formed by a NOD-like receptor (NLR) sensor component (i.e. cryopyrin [NLRP3 or NALP3]), an adaptor component (ASC), an effector component (caspase-1) and the substrate component (the pro-inflammatory cytokines pro-IL-1β and pro-IL-18). The sensors recognize danger signals such as Damage associated molecular pattern molecules (DAMPs) released during tissue injury or stress (extracellular ATP, urate crystal, β-amyloid, cell debris) and Pathogen-associated molecular patterns (PAMPs), evolutionary conserved structures of infectious pathogens. Among the NLR family members, cryopyrin (NLRP3 or NALP3) is the most studied inflammasome sensor. The assembly of the inflammasome requires the interaction of the pyrin domains of cryopyrin and the ...

Sulfone sulfonylimide combinations for advanced battery chemistries

Disclosed is an electrochemical cell, which may be used for advanced rechargeable batteries. The electrochemical cell comprises two or more electrodes within an electrolyte solution, where the electrolyte solution containing (i) an aliphatic or cyclic sulfone and (ii) a metal perfluoroalkylsulfonylimide salt.

N-PHENYL-N'-PHENOXYCARBONYL-PHENYLSULFONHYDRAZIDE DERIVATIVE AND PHARMACEUTICAL COMPOSITION COMPRISING THE SAME

The present invention relates to a N-phenyl-N′-phenoxycarbonyl-phenylsulfonhydrazide derivative with excellent inhibitory activity on PGEproduction, a method for preparing the same and a pharmaceutical composition comprising the same as an active ingredient. The present N-phenyl-N′-phenoxycarbonyl-phenylsulfonhydrazide derivative may be used effectively for preventing or treating inflammation, arthritis, high fever, pain, cancer, stroke or bone disease. 2. The N-phenyl-N′-phenoxycarbonyl-phenylsulfonhydrazide derivative according to or pharmaceutically acceptable salt thereof claim 1 ,wherein,{'sup': '1', 'sub': 1', '6, 'Ris hydrogen or C-Calkyl,'}{'sup': '2', 'sub': 1', '6', '1', '6', '1', '6, 'Ris C-Calkyl, C-Calkoxy, halogen, C-Chaloalkyl or aryl,'}{'sup': '3', 'sub': 1', '6, 'Ris hydrogen or C-Calkyl,'}{'sup': '4', 'sub': 1', '6, 'Ris hydrogen or C-Calkoxy,'}{'sup': '5', 'Ris hydrogen, and'}{'sup': '6', 'sub': 1', '6', '1', '6, 'Ris hydrogen, C-Calkyl, C-Calkoxy or aryloxy, or'}{'sup': 5', '6, 'Rand Rare taken together with the carbon atom to which they are attached to form a 4 to 7-membered hydrocarbon ring.'}3. The N-phenyl-N′-phenoxycarbonyl-phenylsulfonhydrazide derivative according to or pharmaceutically acceptable salt thereof claim 1 ,wherein,{'sup': '1', 'Ris hydrogen or methyl,'}{'sup': '2', 'Ris methyl, n-propyl, i-propyl, t-butyl, methoxy, chloro, trifluoromethyl or phenyl,'}{'sup': '3', 'Ris hydrogen or methyl,'}{'sup': '4', 'Ris hydrogen or methoxy,'}{'sup': '5', 'Ris hydrogen, and'}{'sup': '6', 'Ris hydrogen, methyl, ethyl, methoxy, ethoxy, phenoxy or benzyloxy, or'}{'sup': 5', '6, 'Rand Rare taken together with the carbon atom to which they are attached to form a 5-membered hydrocarbon ring.'}4. The N-phenyl-N′-phenoxycarbonyl-phenylsulfonhydrazide derivative according to or pharmaceutically acceptable salt thereof selected from the group consisting of the following compounds:N-phenyl-N′-(4-methoxyphenoxycarbonyl)-4-methoxyphenylsulfonhydrazide (I ...

COMPOUNDS CONTAINING A SULFONIC GROUP AS KAT INHIBITORS

The present invention provides compounds, pharmaceutically acceptable compositions thereof, and methods of using the same. 2. The compound according to claim 1 , wherein L is a 3-atom linker.4. The compound according to claim 1 , wherein L is a 4-atom linker.6. (canceled)7. The compound according to claim 1 , wherein L is a 5-atom linker.9. The compound according to claim 1 , wherein Z is optionally substituted Caliphatic.10. (canceled)11. The compound according to claim 1 , wherein Z is —Cy.1214-. (canceled)15. The compound according to claim 1 , wherein Ring B is an optionally substituted 3-7 membered saturated or partially unsaturated heterocyclic ring having 1-2 heteroatoms independently selected from nitrogen claim 1 , oxygen and sulfur.1622-. (canceled)23. The compound according to claim 1 , wherein Ring A is phenyl.24. The compound according to claim 1 , wherein Ring A is a 8-10 membered bicyclic heteroaryl ring having 1-3 heteroatoms independently selected from nitrogen oxygen and sulfur.25. The compound according to claim 1 , wherein Ring A is a 3-7 membered saturated or partially unsaturated heterocyclic ring having 1-2 heteroatoms independently selected from nitrogen claim 1 , oxygen and sulfur.28. A pharmaceutical composition comprising a compound or pharmaceutically acceptable salt thereof according to claim 1 , and a pharmaceutically acceptable excipient.29. A method of treating a disease or disorder associated with KAT-5 in a subject in need thereof claim 1 , comprising administering to the subject an effective amount of a compound or pharmaceutically acceptable salt thereof according to .30. A method of modulating protein acetylation in a subject in need thereof claim 1 , comprising administering to the subject an effective amount of a compound or pharmaceutically acceptable salt thereof according to .31. A method of treating cancer in a subject claim 1 , comprising administering to the subject an effective amount of a compound or pharmaceutically ...

N-substituted isopropyldimethyl azulene sulfonamide derivatives, and preparation method and use thereof

The present invention provides an N-substituted isopropyldimethyl azulene sulfonamide derivative as represented by formula (I), and preparation method and uses thereof, wherein R1 is an alkyl, cycloalkyl, alkenyl, alkynyl, aryl, heteroaryl, amino, or a substituted alkyl, cycloalkyl, alkenyl, alkynyl, aryl, heteroaryl, and amino. The N-substituted isopropyldimethyl azulene sulfonamide derivative can be used in treating gastric ulcer.

A developing agent precursor for laser markable compositions

Developing agent precursors and laser markable compositions including such developing agent precursors.

SULFONYL SEMICARBAZIDES, SEMICARBAZIDES AND UREAS, PHARMACEUTICAL COMPOSITIONS THEREOF, AND METHODS FOR TREATING HEMORRHAGIC FEVER VIRUSES, INCLUDING INFECTIONS ASSOCIATED WITH ARENAVIRUSES

Compounds, methods and pharmaceutical compositions for treating viral infections, by administering certain novel semicarbazides, sulfonyl carbazides, ureas and related compounds in therapeutically effective amounts are disclosed. Methods for preparing the compounds and methods of using the compounds and pharmaceutical compositions thereof are also disclosed. In particular, the treatment and prophylaxis of viral infections such as caused by hemorrhagic fever viruses is disclosed, i.e., including but not limited to Arenaviridae (Junin, Machupo, Guanavito, Sabia and Lassa), Filoviridae (ebola and Marburg viruses), Flaviviridae (yellow fever, omsk hemorrhagic fever and Kyasanur Forest disease viruses), and Bunyaviridae (Rift Valley fever). 134-. (canceled)38. A pharmaceutical composition of claim 35 , wherein n is 0 or 1.39. A pharmaceutical composition of claim 35 , wherein n is 0.40. A pharmaceutical composition of claim 35 , wherein m is 1 and p is 1.41. A pharmaceutical composition of claim 35 , wherein m is 0 and p is 0.44. A pharmaceutical composition of claim 35 , wherein the compound of formula I is selected from the group consisting of:N-2-(1,1,1,3,3,3-Hexafluoro-2-methylpropyl)-2-[4-(phenyl)-phenylsulfonyl]hydrazine-1-carboxamide;N-2-(1,1,1,3,3,3-Hexafluoro-2-methylpropyl)-2-[4-(2-methyl-2-propyl)-phenylsulfonyl]hydrazine-1-carboxamide;N-2-(1,1,1,3,3,3-Hexafluoro-2-methylpropyl)-2-[7-(4-methyl-3,4-dihydro-2H-benzo[1,4]oxazinyl)sulfonyl]hydrazine-1-carboxamide;N-2-(1,1,1,3,3,3-Hexafluoro-2-methylpropyl)-2-[5-(1-dimethylamino-naphthyl) sulfonyl]hydrazine-1-carboxamide; N-2-(1,1,1,3,3,3-Hexafluoro-2-methylpropyl)-2-[(2,4,6-trimethylphenyl)sulfonyl]hydrazine-1-carboxamide;N-2-(1,1,1,3,3,3-Hexafluoro-2-methylpropyl)-2-[(3-chloro-6-methoxyphenyl) sulfonyl]hydrazine-1-carboxamide;N-2-(1,1,1,3,3,3-Hexafluoro-2-methylpropyl)-2-[(3,6-dimethoxyphenyl)sulfonyl]hydrazine-1-carboxamide;N-2-(1,1,1,3,3,3-Hexafluoro-2-methylpropyl)-2-[(4-(4-[1,2,3]thiadiazolyl) phenyl)sulfonyl ...

ARYL SULFONOHYDRAZIDES

Compound of formula I: 3: A compound according to claim 1 , wherein Ris H.4: A compound according to claim 1 , wherein Ris F.5: A compound according to claim 1 , wherein none of X claim 1 , X claim 1 , Xand Xare N.7: A compound according to claim 1 , wherein one of X claim 1 , X claim 1 , Xand Xis N.8: A compound according to claim 1 , wherein Ris I.9: A compound according to claim 1 , wherein Ris unsubstituted phenyl.10: A compound according to claim 1 , wherein Ris phenyl substituted by a single substituent selected from halo claim 1 , cyano and Calkoxy.11: A compound according to claim 10 , where the substituent is halo and is selected from F and Cl.12: A compound according to claim 10 , where the substituent is cyano.13: A compound according to claim 10 , where the substituent is methoxy.15: A compound according to claim 1 , wherein Ris optionally substituted Calkyl claim 1 , and is selected from methyl claim 1 , ethyl claim 1 , iso-propyl and CF.17: A pharmaceutical composition comprising a compound according to claim 1 , and a pharmaceutically acceptable excipient.18: (canceled)19: A method of treatment of cancer claim 1 , comprising administering to a patient in need of treatment claim 1 , a compound according to .2021-: (canceled)22: A method of treatment of a condition ameliorated by the inhibition of MOZ claim 1 , comprising administering to a patient in need of treatment claim 1 , a compound according to .2324-: (canceled) The present invention relates to aryl sulfonohydrazides, their use as pharmaceuticals, and in particular, in treating cancer and other diseases associated with the inhibition of MOZ and/or QKF.There are approximately 31,000 new cases of leukaemia diagnosed in the USA per year and approximately 22,000 deaths (Jemal et al 2002). Leukaemia can be divided into acute forms (e.g. acute myeloid leukaemia: AML), characterised by the presence of excessive numbers of immature leukocytes and chronic forms (e.g. chronic myeloid leukaemia: CML), ...

FLUOROALLYLSULFONYL AZIDE MONOMERS AND POLYMERS THERE FROM

This invention pertains to fluoroallylsulfonyl azide compounds of formula: CF═CF—CF—R—SONformula (I) wherein Ris a divalent (per)fluorinated group, optionally comprising one or more than one ethereal oxygen atom [monomer (Az)], which are useful as functional monomers in fluoropolymers, to the fluoropolymers which comprise recurring units derived from such fluoroallylsulfonyl azide compounds, to a process for their manufacture, to a curable compound comprising the same and to a method for crosslinking the same. 1. A sulfonyl azide allylic monomer of formula (I):{'br': None, 'sub': 2', '2', 'f', '2', '3, 'CF═CF—CF—O—R—SON\u2003\u2003(I)'}{'sub': 'f', 'wherein Ris a divalent (per)fluorinated group, optionally comprising one or more than one ethereal oxygen atom.'}2. The monomer of claim 1 , wherein said monomer is a monomer of formula (Ia):{'br': None, 'sub': 2', '2', '2', 'f', '2', '3, 'CF═CF—CF—O—CF—R′—SON\u2003\u2003(Ia),'}{'sub': f', '1', '12, 'wherein R′ is a divalent C-C(per)fluorinated group, optionally comprising one or more than one ethereal oxygen atom.'}3. The monomer of claim 2 , wherein said monomer is a monomer of formula (Ib):{'br': None, 'sub': 2', '2', '2', '2', '2', '3, 'CF═CF—CF—O—CF—CF—SON\u2003\u2003(Ib).'}4. A process for the manufacture of a monomer of claim 1 , comprising reacting a fluorosulfonic precursor of formula (II):{'br': None, 'sub': 2', '2', 'f', '2, 'CF═CF—CF—O—R—SO\u2003\u2003(II)'}{'sub': 'f', 'wherein Ris a divalent (per)fluorinated group, optionally comprising one or more than one ethereal oxygen atom,'}with an azide salt.5. A fluoropolymer comprising recurring units derived from at least one monomer of formula (I):{'br': None, 'sub': 2', '2', 'f', '2', '3, 'CF═CF—CF—O—R—SON\u2003\u2003(I)'}{'sub': 'f', 'wherein Ris a divalent (per)fluorinated group, optionally comprising one or more than one ethereal oxygen atom,'}and, optionally, recurring units derived from at least one ethylenically unsaturated fluorinated monomer different ...

CHEMICAL FOAMING AGENTS CONTAINING TOSYL GROUPS

Chemical foaming agents having p-toluenesulfonyl groups. Processes for preparing foamed polyolefin compositions using chemical foaming agents having p-toluenesulfonyl groups. Articles of manufacture containing formed polyolefins prepared using chemical foaming agents having p-toluenesulfonyl groups. 2. The chemical foaming agent of claim 1 , comprising one or more of the compounds shown as structures (I) through (III).3. The chemical foaming agent of claim 1 , consisting of one or more of the compounds shown as structures (I) through (III).4. A foamable polyolefin composition comprising a polyolefin and the chemical foaming agent of .5. The foamable polyolefin composition of claim 4 , wherein the polyolefin comprises an ethylene-based polymer claim 4 , wherein the foamable polyolefin composition further comprises an additive selected from the group consisting of antioxidants claim 4 , cell stabilizers claim 4 , and combinations thereof.6. A foamed polyolefin prepared from the foamable polyolefin composition of .7. A cable comprising an insulation layer claim 6 , wherein the insulation layer comprises the foamed polyolefin of .9. The process of claim 8 , wherein the chemical foaming agent is present in an amount ranging from 0.1 to 1.0 weight percent claim 8 , based on the total weight of the foamable polyolefin composition claim 8 , wherein the polyolefin comprises an ethylene-based polymer claim 8 , wherein the polyolefin is present in an amount ranging from 90 to 99.9 weight percent claim 8 , based on the total weight of the foamable polyolefin composition.10. The process of claim 9 , wherein the foamable polyolefin composition further comprises an additive selected from the group consisting of antioxidants claim 9 , cell stabilizers claim 9 , and combinations thereof. Various embodiments relate to chemical foaming agents containing tosyl groups. Additional embodiments relate to employing tosyl-group-containing chemical foaming agents in foamable polyolefin ...

Chemical inducers of neurogenesis

The present invention relates to compounds and methods for inducing neuronal differentiation in normal neural stem cells and brain cancer stem cells. The methods may take place in vitro, such as in isolates from the adult mammalian brain, or in vivo. Compounds and methods described herein may find use in the treatment of neurodegenerative and psychiatric diseases, the repair and regeneration of the nervous system, and in treatment of neurologic malignancy.

NOVEL COMPOUNDS

Compounds of the formula (I), in which the substituents are as defined in claim , are suitable for use as nematicides. 2. The nematicidal composition according to claim 1 , wherein A is a 6-membered heteroaryl containing 1 to 2 nitrogen atoms claim 1 , or phenyl claim 1 , wherein the heteroaryl or the phenyl ring is substituted by one or more R claim 1 , where{'sub': '6', 'Ris, independently of each other, from halogen, cyano, C1-C4-alkyl, C1-C4-haloalkyl, and C1-C4-haloalkoxy,'}{'sub': 1', '2', '3, 'Ris hydrogen, halogen or C1-C4-alkyl, Rand Ris, independently of each other, hydrogen or C1-C4-alkyl,'}{'sub': 4', '5, 'Rand Rare each hydrogen,'}B is a 6 membered heteroaromatic ring containing 1 nitrogen atom, or a mono-5 to 10 membered aromatic ring system, wherein the heteroaromatic ring or the aromatic ring system is substituted by one or more R9, whereR9 is, independently of each other, halogen, cyano, R8, —OR8, —S(O)nR8, where n is 0, 1, or 2, andR8 is, independently of each other, C1-C4-alkyl, which is unsubstituted or substituted by R10, C3-C6-cycloalkyl, which is unsubstituted or substituted by R10, phenyl, which is unsubstituted or substituted by R10 or heteroaryl, which is unsubstituted or substituted by R10, whereR10 is halogen, cyano, or C1-C4-haloalky; provided where R8 is heteroaryl, R10 is halogen, cyano, C1-C4-alkyl, C1-C4-haloalkyl, C1-C4-alkoxy, C1-C4-haloalkoxy, C1-C4-alkylthio, C1-C4-alkylcarbonyl, or C1-C4alkoxycarbonyl,wherein B and A-CO—NR5 are cis to each other on the cyclopropyl ring.3. The nematicidal composition according to claim 2 , wherein A is a 6-membered heteroaryl containing 1 or 2 nitrogen atoms claim 2 , or phenyl claim 2 , wherein the heteroaryl or the phenyl ring is substituted by one or more R claim 2 , where{'sub': '6', 'Ris, independently of each other, from halogen, cyano, C1-C4-alkyl, C1-C4-haloalkyl, and C1-C4-haloalkoxy,'}{'sub': '1', 'Ris hydrogen or halogen,'}{'sub': 2', '3, 'Rand Ris, independently of each other, ...

SULFONYL SEMICARBAZIDES, SEMICARBAZIDES AND UREAS,PHARMACEUTICAL COMPOSITIONS THEREOF, AND METHODS FOR TREATING HEMORRHAGIC FEVER VIRUSES, INCLUDING INFECTIONS ASSOCIATED WITH ARENAVIRUSES

Compounds, methods and pharmaceutical compositions for treating viral infections, by administering certain novel semicarbazides, sulfonyl carbazides, ureas and related compounds in therapeutically effective amounts are disclosed. Methods for preparing the compounds and methods of using the compounds and pharmaceutical compositions thereof are also disclosed. In particular, the treatment and prophylaxis of viral infections such as caused by hemorrhagic fever viruses is disclosed, i.e., including but not limited to Arenaviridae (Junin, Machupo, Guanavito, Sabia and Lassa), Filoviridae (ebola and Marburg viruses), Flaviviridae (yellow fever, omsk hemorrhagic fever and Kyasanur Forest disease viruses), and Bunyaviridae (Rift Valley fever). 16.-. (canceled)7. A compound selected from the group consisting of: 1-[1 ,1-bis(trifluoromethyl)propyl]-3-[(2 ,4 ,6-trimethylphenyl)sulfonylamino]urea;1-[1,1-bis(trifluoromethyl)propyl]-3-[(4-tert-butylphenyl)sulfonylamino]urea;1-[1,1-bis(trifluoromethyl)propyl]-3-[(2,5-dimethoxyphenyl)sulfonylamino]urea;1-[1,1-bis(trifluoromethyl)propyl]-3-(2-naphthylsulfonylamino)urea;1-[1,1-bis(trifluoromethyl)propyl]-3-[(4-isopropylphenyl)sulfonylamino]urea;1-[1,1-bis(trifluoromethyl)propyl]-3-[(5-chloro-2-methoxy-phenyl)sulfonylamino]urea;1-[1,1-bis(trifluoromethyl)propyl]-3-[(2-phenylphenyl)sulfonylamino]urea;1-[1,1-bis(trifluoromethyl)propyl]-3-[(3,4-dichlorophenyl)sulfonylamino]urea;1-[1,1-bis(trifluoromethyl)propyl]-3-[(4-bromophenyl)sulfonylamino]urea;1-[1,1-bis(trifluoromethyl)propyl]-3-[[4-(difluoromethoxy)phenyl]sulfonylamino]urea;1-[1,1-bis(trifluoromethyl)propyl]-3-[(3,5-dimethylphenyl)sulfonylamino]urea;1-[1,1-bis(trifluoromethyl)propyl]-3-[[5-(dimethylamino)-1-naphthyl]sulfonylamino]urea;1-[1,1-bis(trifluoromethyl)propyl]-3-(1-naphthylsulfonylamino)urea;1-[1,1-bis(trifluoromethyl)propyl]-3-[(4-methyl-2,3-dihydro-1,4-benzoxazin-7-yl)sulfonylamino]urea;1-[[2,5-bis(2,2,2-trifluoroethoxy)phenyl]sulfonylamino]-3-[1,1-bis(trifluoromethyl) ...

MONOMER, POLYMER, RESIST COMPOSITION, AND PATTERNING PROCESS

A monomer having an onium salt structure represented by formula (1) gives a polymer which is fully compatible with resist components. A resist composition comprising the polymer has advantages including reduced acid diffusion, high sensitivity, high resolution, a good balance of lithography properties, and less defects, and is quite effective for precise micropatterning. 3. The monomer of wherein Lis a sulfonyl bond.4. The monomer of wherein Lis a single bond and Ais hydrogen claim 1 , fluorine or trifluoromethyl.5. A polymer comprising recurring units derived from the monomer of .7. The polymer of wherein Lis a sulfonyl bond.8. The polymer of wherein Lis a single bond and Ais hydrogen claim 6 , fluorine or trifluoromethyl.9. A resist composition comprising a base resin containing the polymer of and an organic solvent.13. The resist composition of claim 9 , further comprising an amine compound.15. The resist composition of claim 9 , further comprising a surfactant which is insoluble or substantially insoluble in water and soluble in alkaline developer claim 9 , and/or a surfactant which is insoluble or substantially insoluble in water and alkaline developer.16. A pattern forming process comprising the steps of applying the resist composition of onto a substrate claim 9 , prebaking to form a resist film claim 9 , exposing a selected region of the resist film to KrF excimer laser claim 9 , ArF excimer laser claim 9 , EB or EUV claim 9 , baking claim 9 , and developing the exposed resist film in a developer.17. The pattern forming process of wherein the developing step uses an alkaline aqueous solution as the developer claim 16 , thereby forming a positive pattern in which an exposed region of the resist film is dissolved away and an unexposed region of the resist film is not dissolved.18. The pattern forming process of wherein the developing step uses an organic solvent as the developer claim 16 , thereby forming a negative pattern in which an unexposed region of the ...

Lipoic acid derivatives and their use in treatment of disease

Chemical foaming agents containing tosyl groups

Chemical foaming agents having p-toluenesulfonyl groups. Processes for preparing foamed polyolefin compositions using chemical foaming agents having p-toluenesulfonyl groups. Articles of manufacture containing formed polyolefins prepared using chemical foaming agents having p-toluenesulfonyl groups.

含有甲苯磺酰基的化学发泡剂

一种具有对甲苯磺酰基的化学发泡剂。一种使用具有对甲苯磺酰基的化学发泡剂制备发泡聚烯烃组合物的方法。使用具有对甲苯磺酰基的化学发泡剂制备的含有成型聚烯烃的制品。

Chemical agents capable of forming covalent 3-d networks

본 발명은 동일하거나 다른, n개의 카르벤 전구체기를 포함하는 식(II)의 관능성 화합물을 제공하고, 여기서 n은 3 이상의 정수이며: x는 1이고, E는 카르벤 반응 중간체기로 전환될 수 있는 기이며, Q는 중심부, 폴리머 또는 덴드리머이고, 각각의 [R] x -E-L- 기는 동일하거나 다르며 식(Ie)의 기 및 식(Ia)의 기로부터 선택된다: 여기서 L은 본원에 정의된 단결합 또는 연결기이고, R은 본원에 정의된 말단기이고, R 1 은 본원에 정의되어 있다. 기판상 또는 내에 화학적으로 결합된 3차원 네트워크를 제조하기 위한 제제로서 관능성 화합물의 사용을 제공한다. 본 발명의 관능성 화합물을 사용하여 하기의 제품을 제조하는 방법을 하기와 같이 제공한다: 기판상 또는 내에 화학적으로 결합된 3차원 네트워크; 제 1 기판과 제 2 기판 사이에 화학적으로 결합된 3차원 네트워크; 필름 또는 코팅; 코팅된 기판; 제 1 기판, 제 2 기판, 및 제 1 기판과 제 2 기판의 계면에서 조성물을 포함한 제품; 처리된 입자. 본 발명은 본 발명의 관능성 화합물을 사용하여 제1 기판 내지 제 2 기판을 가교결합하기 위한 방법 및 얻어진 가교제품을 제공한다. 본 발명은 관능성 화합물의 제조방법을 제공한다. The present invention provides the same or different functional compounds of formula (II) comprising n carbene precursor groups, wherein n is an integer greater than or equal to 3: X is 1, E is a group which can be converted to a carbene reactive intermediate group, Q is a central part, polymer or dendrimer, each [R] x -EL- group is the same or different and is a group of formula (Ie) Lt; RTI ID = 0.0 &gt; Ia) &lt; / RTI & Wherein L is a single bond or linking group as defined herein, R is a terminal group as defined herein and R &lt; 1 &gt; is defined herein. Provides the use of a functional compound as a formulation for making a three-dimensional network chemically bonded onto or within a substrate. A method for producing the following products using the functional compounds of the present invention is provided as follows: a three dimensional network chemically bonded onto or within a substrate; A three-dimensional network chemically coupled between the first substrate and the second substrate; Film or coating; A coated substrate; A product comprising a first substrate, a second substrate, and a composition at an interface between the first substrate and the second substrate; Treated particles. The present invention provides a method for crosslinking a first substrate to a second substrate using the functional compound of the present ...

具有杀虫效用的分子，以及与这些分子相关的中间体、组合物和方法

本公开涉及以下领域：对节肢动物门、软体动物门和线虫动物门中的害虫具有杀虫效用的分子，制备此类分子的方法，用于此类方法的中间体，含有此类分子的组合物，以及使用此类分子和组合物对抗此类害虫的方法。这些分子和组合物可以用作例如杀螨剂、杀昆虫剂、杀疥虫剂、杀软体动物剂和杀线虫剂。本文件公开了具有下式(“式1”)的分子。

Lipoic acid derivatives and their use in the treatment of diseases

Compounds for treatment of proliferative disorders

FIELD: medicine, pharmaceutics. SUBSTANCE: claimed invention relates to novel compounds of formula (V), compounds of formula (IX), compounds of formula (XIII) or their tautomers or pharmaceutically acceptable salts, which are capable of inducing Hsp70, as well as to pharmaceutical composition, which contains claimed compounds. Value of substituents in formulas (V), (IX) and (XIII) are such, as claimed in invention formula. EFFECT: obtaining pharmaceutically acceptable salts, which have possibility of inducing Hsp70. 12 cl, 12 ex, 36 dwg, 2 tbl РОССИЙСКАЯ ФЕДЕРАЦИЯ (19) RU (11) 2 475 478 (13) C2 (51) МПК C07C C07C C07C C07C C07C C07C C07D ФЕДЕРАЛЬНАЯ СЛУЖБА ПО ИНТЕЛЛЕКТУАЛЬНОЙ СОБСТВЕННОСТИC07D C07D C07D (12) ОПИСАНИЕ 327/56 307/04 311/49 337/06 317/28 243/28 207/34 263/48 271/10 307/38 (2006.01) (2006.01) (2006.01) (2006.01) (2006.01) (2006.01) (2006.01) (2006.01) (2006.01) (2006.01) C07F A61K A61K A61P ИЗОБРЕТЕНИЯ К ПАТЕНТУ (72) Автор(ы): ЧЭНЬ Шоуцзюнь (US), КОЯ Кейзо (US), ДЕМКО Закари (US), СУНЬ Лицзюнь (US) (21)(22) Заявка: 2009109949/04, 20.08.2007 (24) Дата начала отсчета срока действия патента: 20.08.2007 (73) Патентообладатель(и): СИНТА ФАРМАСЬЮТИКЛЗ КОРП. (US) (45) Опубликовано: 20.02.2013 Бюл. № 5 (56) Список документов, цитированных в отчете о поиске: US 2003/195258 А1, 16.10.2003. US 6656971 B2, 02.12.2003. SU 687069 A, 25.09.1979. (86) Заявка PCT: US 2007/018378 (20.08.2007) C 2 C 2 (85) Дата начала рассмотрения заявки PCT на национальной фазе: 23.03.2009 2 4 7 5 4 7 8 (87) Публикация заявки РСТ: WO 2008/024303 (28.02.2008) R U 2 4 7 5 4 7 8 (43) Дата публикации заявки: 27.09.2010 Бюл. № 27 R U Приоритет(ы): (30) Конвенционный приоритет: 21.08.2006 US 60/839,034 31.08.2006 US 60/841,408 Адрес для переписки: 119011, Москва, Гоголевский б-р, 11, Гоулингз Интернэшнл Инк., А.Ю. Соболеву (54) СОЕДИНЕНИЯ ДЛЯ ЛЕЧЕНИЯ ПРОЛИФЕРАТИВНЫХ РАССТРОЙСТВ (57) Реферат: Настоящее изобретение относится к новым соединениям формулы (V), соединениям формулы (IX), соединениям ...

Guanidine compounds and use thereof

Sulfated amino acid derivatives and metalloproteinase inhibitors comprising thereof

FIELD: medicine, biochemistry, enzymology. SUBSTANCE: invention relates to pharmaceutical composition used for inhibition of metalloproteinase activity comprising sulfated amino acid derivatives and novel sulfated derivatives of amino acids. EFFECT: enhanced activity of compositions. 26 cl, 54 tbl Эб5эз6тгс пы сэ РОССИЙСКОЕ АГЕНТСТВО ПО ПАТЕНТАМ И ТОВАРНЫМ ЗНАКАМ (19) ВО ‘”2 198 656 ' 5 МК’ А 64 К 31/18, С 07 С 311/00, А 13) С2 61Р 29/00, 35/04, 19/10 12) ОПИСАНИЕ ИЗОБРЕТЕНИЯ К ПАТЕНТУ РОССИЙСКОЙ ФЕДЕРАЦИИ (21), (22) Заявка: 98115659/14, 22.01.1997 (24) Дата начала действия патента: 22.01.1997 (30) Приоритет: 23.01.1996 УР 8/30082 13.08.1996 УР 8/213555 (43) Дата публикации заявки: 27.06.2000 (46) Дата публикации: 20.02.2003 (56) Ссылки: ЕР 0468231 А2, 29.01.1992. МО 93/14069 А, 22.07.1993. ММО 96/00214 А, 04.01.1996. КЦ 2132327 СЛ, 27.06.1999. (85) Дата перевода заявки РСТ на национальную фазу: 24.08.1998 (86) Заявка РСТ: УР 9700126 (22.01.1997) (87) Публикация РСТ: М/О 97/27174 (31.07.1997) (98) Адрес для переписки: 101000, Москва, М.Златоустинский пер., д.10, кв.15, "ЕВРОМАРКПАТ", Н.В.Кузенковой (71) Заявитель: ШИОНОГИ ЭНД КО., ЛТД. (4Р) (72) Изобретатель: ВАТАНАБЕ Фумихико (/Р), ТСУЗУКИ Хирошиге (.Р), ОХТАНИ Митсуаки (УР) (73) Патентообладатель: ШИОНОГИ ЭНД КО., ЛТД. (Р) (74) Патентный поверенный: Веселицкая Ирина Александровна (54) СУЛЬФИРОВАННЫЕ АМИНОКИСЛОТНЫЕ ПРОИЗВОДНЫЕ И СОДЕРЖАЩИЕ ИХ ИНГИБИТОРЫ МЕТАЛЛОПРОТЕИНАЗ (57) Изобретение относится к области медицины и касается фармкомпозиции для ингибирования металлопротеиназы, содержащей сульфированные аминокислотные производные, и новых сульфированных аминокислотных производных. Композиции обладают повышенной активностью. 8 с. и 18 з.п. ф-лы, 54 табл. 2198656 С2 КО (19) 13) ВИ "” 2 4198 656 ^С2 А 64 К 31/48, С 07 С 311/00, А 61Р 29/00, 35/04, 19/10 Эб5эз6тгс пы сэ КУЗЗАМ АСЕМСУ ГОК РАТЕМТ$ АМО ТКАОЕМАКК$ 12) АВЗТКАСТ ОЕ 1МУЕМТОМ (21), (22) АррИсаНоп: 98115659/14, 22.01.1997 (24) ЕНесНуе дае Гог ргорейу па: 22.01. ...

Guanidine compounds and use thereof

본 발명은 미토콘드리아의 산화적 인산화 (OXPHOS)를 억제하기 위한 구아니딘 화합물 및 그의 용도에 관한 것이다. 보다 구체적으로, 본 발명은 미토콘드리아의 산화적 인산화를 억제하고 세포 대사를 재프로그래밍함으로써 OXPHOS와 관련된 질환, 특히 암을 예방 또는 치료하기 위한 약학 조성물에 관한 것이다. The present invention relates to guanidine compounds and their use for inhibiting oxidative phosphorylation (OXPHOS) of mitochondria. More specifically, the present invention relates to pharmaceutical compositions for preventing or treating diseases associated with OXPHOS, in particular cancer, by inhibiting oxidative phosphorylation of mitochondria and reprogramming cell metabolism.

Insecticidal phenylhydrazine derivatives

아래의 구조식을 갖는 화합물이 개시된다: Compounds having the structure below are disclosed: 여기서 X, Y, R 및 Z는 명세서에 정의된 바와 같다. 본 발명의 화합물은 진드기, 선충류, 벼 메뚜기, 담배 싹병 및 사우턴 옥수수 뿌리병을 구제하는데 유용하다. 이들 화합물의 제법도 제시된다. Wherein X, Y, R and Z are as defined in the specification. The compounds of the present invention are useful for controlling ticks, nematodes, rice locusts, tobacco shoots and Southern corn root disease. The preparation of these compounds is also shown.

Hydrazine derivatives

하기 화학식 I의 하이드라진 유도체 또는 그의 약학적으로 허용가능한 염은 세포로부터 종양 괴사 인자(TNF-α) 및 형질전환 성장 인자(TGF-α)의 방출을 억제할 뿐 아니라, 케라티노사이트 증식을 억제한다: Hydrazine derivatives of formula (I) or pharmaceutically acceptable salts thereof, inhibit not only the release of tumor necrosis factor (TNF-α) and transforming growth factor (TGF-α) from cells, but also inhibit keratinocyte proliferation : 화학식 I Formula I 상기 식에서, Where Y는 CO 또는 SO 2 를 의미하고; Y means CO or SO 2 ; R 1 은 저급 알킬, 저급 알케닐, 저급 사이클로알킬, 저급 사이클로알킬-저급 알킬, 아릴 또는 아릴-저급 알킬을 의미하고; R 1 means lower alkyl, lower alkenyl, lower cycloalkyl, lower cycloalkyl-lower alkyl, aryl or aryl-lower alkyl; R 2 는 Y가 SO 2 를 의미하는 경우에는 저급 알킬, 할로-저급 알킬, 아릴-저급 알킬, 아릴-저급 알케닐 또는 아릴을 의미하고, Y가 CO를 의미하는 경우에는 저급 알킬, 할로-저급 알킬, 저급 알콕시, 저급 알콕시카보닐, 아실, 저급 사이클로알킬, 아릴, 아릴-저급 알킬, 아릴-저급 알콕시 또는 NR 5 R 6 를 의미하며; R 2 means lower alkyl, halo-lower alkyl, aryl-lower alkyl, aryl-lower alkenyl or aryl when Y means SO 2, and lower alkyl, halo-lower when Y means CO Alkyl, lower alkoxy, lower alkoxycarbonyl, acyl, lower cycloalkyl, aryl, aryl-lower alkyl, aryl-lower alkoxy or NR 5 R 6 ; R 3 는 수소, R 3 is hydrogen, 시아노, 아미노, 하이드록시, 저급 알콕시, 저급 알콕시카보닐, 헤테로사이클릴 또는 헤테로사이클릴카보닐로 치환되거나 비치환된 저급 알킬, Lower alkyl unsubstituted or substituted with cyano, amino, hydroxy, lower alkoxy, lower alkoxycarbonyl, heterocyclyl or heterocyclylcarbonyl, 저급 알케닐, 저급 알키닐, 저급 사이클로알킬, 저급 사이클로알킬-저급 알킬, 아릴-저급 알킬, 아릴-저급 알케닐, 아릴 또는 헤테로사이클릴이거나; 또는 Lower alkenyl, lower alkynyl, lower cycloalkyl, lower cycloalkyl-lower alkyl, aryl-lower alkyl, aryl-lower alkenyl, aryl or heterocyclyl; or R 2 및 R 3 는 함께 5-, 6- 또는 7-원 환형 아미드, 환형 이미드, 환형 설폰아미드 또는 환형 우레탄 그룹의 잔기를 형성하고; R 2 and R 3 together form a residue of a 5-, 6- or 7-membered cyclic amide, cyclic imide, cyclic sulfonamide or cyclic urethane group; R 4 는 저급 알킬, 하이드록시-저급 알킬, 저급 알케닐, 저급 사이클로알킬, 저급 사이클로알킬-저급 알킬 또는 일반식 X-아릴, X-헤테로아릴 또는 -(CH 2 ) 1-2 -CH=CR 7 R 8 의 그룹을 의미하며; R 4 is lower alkyl, hydroxy-lower alkyl, lower alkenyl, lower cycloalkyl, lower cycloalkyl-lower alkyl or a general ...

Androgen receptor modulators and methods for their use

Compounds having a structure of formula (I), (I-A), (Ia)-(Ie), (A)-(E), and (II) or a pharmaceutically acceptable salt, tautomer or stereoisomer thereof are provided. Uses of such compounds for modulating androgen receptor activity, imaging diagnostics in cancer and therapeutics, and methods for treatment of disorders including prostate cancer are also provided.

Sulfonated amino acid derivatives and metalloproteinase inhibitors containing the same

Compounds having a metalloproteinase inhibitory activity, represented by the formula (I), its optically active isomers, their pharmaceutically acceptable salts, or hydrates thereof. (see formula I)

Sulfonated amino acid derivatives and metalloproteinase inhibitors containing the same

Compounds having a metalloproteinase inhibitory activity, represented by the formula (I), its optically active isomers, their pharmaceutically acceptable salts, or hydrates thereof.

Sulfonated derivatives of amino acids and metalloprotease inhibitors in which said derivatives are comprised

In the present invention, there are disclosed amino acid sulfonated derivatives exhibiting a metalloproteinase inhibitory activity, represented by the general formula I, their optically active isomers, their pharmaceutically acceptable salts, and their hydrates.

Sulfonated amino acid derivatives and metalloproteinase inhibitors containing the same

Compounds having a metalloproteinase inhibitory activity, represented by the formula (I), its optically active isomers, their pharmaceutically acceptable salts, or hydrates thereof.

Sulfonated amino acid derivatives and metalloproteinase inhibitors containing the same

Compounds having a metalloproteinase inhibitory activity, represented by the formula (I), its optically active isomers, their pharmaceutically acceptable salts, or hydrates thereof.

Sulfonated amino acid derivatives and metalloproteinase inhibitors containing the same

Compounds having a metalloproteinase inhibitory activity, represented by general formula (I), optically active isomers thereof, or pharmacologically acceptable salts thereof, or hydrates of these.

Insecticidal phenylhydrazine derivatives

具有下述结构式的化合物 其中X，Y，R和Z如公开的具体定义。本发明的化合物可有效地防治螨，线虫，稻飞虱，烟芽叶蛾，和十一星瓜叶甲。还公开了上述化合物的制备方法。

Anthelmintic N'-substituted-N,N'-disubstitutedhydrazines

This invention relates to the anthelmintic use of compositions containing N'-substituted-N,N'-disubstitutedhydrazines. Specifically, the invention relates to methods of controlling helminths by contacting the helminths with a compound having a nucleus of the formula ##STR1## wherein X and X' are the same or different O, S, or NR and A', B', R 1 and R 2 are a variety of substituents.

Detection of cholesterol ozonation products

Glucagon antagonists/inverse agonists

Non-peptide compounds comprising a central hydrazide motif and methods for the synthesis thereof are disclosed. The compounds act to antagonize the action of the glucagon peptide hormone.

Guanidine compounds and uses thereof

Chemical agents capable of forming covalent 3-D networks

本发明提供了式(II)的官能化化合物，该官能化化合物包括相同的或不同的n个卡宾前驱体基团，其中n是等于或大于3的整数：其中x是1，E是能够被转化为卡宾活性中间体基团的基团，Q是核部分、聚合物或树枝状大分子，且相同的或不同的[R] x -E-L-基团中的每一个独立地选自式(Ie)的基团和式(Ia)的基团：其中L是如本文所定义的单键或连接体基团，R是如本文所定义的端基，且R 1 如本文所定义的。还提供了官能化化合物作为用于在基质上或在基质内产生化学上结合的三维网络的剂的用途。还提供了使用本发明的官能化化合物来产生以下产物的方法，以下产物是所得到的产物：在基质上或在基质内的化学上结合的三维网络；在第一基质和第二基质之间的化学上结合的三维网络；膜或涂层；被包覆的基质；包括第一基质、第二基质以及在第一基质和第二基质的界面处的组合物的产物；经处理的颗粒。本发明还提供一种使用本发明的官能化化合物来将第一基质交联于第二基质的方法和所得到的交联产物。本发明还提供一种用于生产本发明的官能化化合物的方法。

Phenol compound and process for preparing the same

披露了一种由式(1)代表的酚化合物：其中，R 0 代表氢原子、可取代的烷基或可取代的烷氧基；R 1 代表可取代的烷基；R 2 代表可取代的烷基或可取代的烷氧基；OR 3 代表可被保护的羟基；R 4 代表氢原子、可取代的低级烷基或可取代的低级酰基；W代表O、S或NR 7 ；其中R 7 代表氢原子、烷基、芳基、羟基或烷氧基、由下式(2)代表的基团：其代表可单-或双-取代的氨基或含有氮原子的杂环基，或其药物学上可接受的盐。

METHOD FOR PRODUCING A LONG CHAIN ALCOHOL OF HIGH CLEANING CYCLOGEXENON

РОССИЙСКАЯ ФЕДЕРАЦИЯ (19) RU (11) (13) 2018 130 292 A (51) МПК C07C 49/753 (2006.01) ФЕДЕРАЛЬНАЯ СЛУЖБА ПО ИНТЕЛЛЕКТУАЛЬНОЙ СОБСТВЕННОСТИ (12) ЗАЯВКА НА ИЗОБРЕТЕНИЕ (21)(22) Заявка: 2018130292, 22.01.2017 (71) Заявитель(и): ТАЙХО ФАРМАСЬЮТИКАЛ КО., ЛТД. (JP) Приоритет(ы): (30) Конвенционный приоритет: 22.01.2016 CN 201610044990.8 (85) Дата начала рассмотрения заявки PCT на национальной фазе: 22.08.2018 R U (43) Дата публикации заявки: 25.02.2020 Бюл. № 6 (72) Автор(ы): ЧЖАН Цзянь (CN), ЦЗЯН Дехуэй (CN), ШЭНЬ Сяоцзюнь (CN) (86) Заявка PCT: (87) Публикация заявки PCT: WO 2017/125087 (27.07.2017) A Адрес для переписки: 129090, Москва, ул. Б. Спасская, 25, стр. 3, ООО "Юридическая фирма Городисский и Партнеры" R U (57) Формула изобретения 1. Способ получения длинноцепочечного спирта циклогексенона высокой чистоты, представленного формулой I, где способ проходит по следующей реакционной схеме: где A является C10-18алкиленом, R1, R2 и R3 каждый независимо является H или метилом, и R4 является H, замещенным или незамещенным C1-7алкилом, замещенным или незамещенным C6-14арилом, или , где замещенный означает замещенный одним заместителем или двумя или более заместителями, выбранными из метила, нитро, хлора и брома; R5 является H, метокси, Стр.: 1 A 2 0 1 8 1 3 0 2 9 2 (54) СПОСОБ ПРОИЗВОДСТВА ДЛИННОЦЕПОЧЕЧНОГО СПИРТА ЦИКЛОГЕКСЕНОНА ВЫСОКОЙ СТЕПЕНИ ОЧИСТКИ 2 0 1 8 1 3 0 2 9 2 CN 2017/072078 (22.01.2017) трет-бутокси, бензилокси, фенилом, 4-метилфенилом или амино; и R4 предпочтительно где способ включает стадии (1a) реакцию конденсации неочищенного продукта длинноцепочечного спирта циклогексенона III и гидразина или его производного R4NHNH2 с получением соединения II, и (1b) гидролиз соединения II в присутствии кислого вещества с получением соединения I высокой чистоты. 2. Способ получения по п. 1, где длинноцепочечный спирт циклогексенон высокой чистоты, представленный формулой I, имеет чистоту по ВЭЖХ более 95%; предпочтительно, длинноцепочечный спирт циклогексенон высокой ...

Organic solvent solution of sulfonimide having polymerizable functional group with reduced halide

본 발명은, 종래의 방법으로는 제조가 어려웠던 할로겐화물이 저감되는 한편, 자연 중합에 대한 안정성이 개량된 중합성 관능기를 갖는 술폰이미드의 저장 등의 형태, 술폰이미드 용액의 제조 방법 및 술폰이미드 용액 중의 할로겐 이온의 제거 방법을 제공한다. 본 발명은, 일반식(1)로 표현되는 술폰이미드의 유기 용제 용액이며, 상기 용액 중의 술폰이미드의 양에 대한 할로겐 이온의 함유량이 1000 ppm 이하인 유기 용제 용액, 술폰이미드 용액의 제조 방법 및 술폰이미드 용액 중의 할로겐 이온의 제거 방법을 이용한다. The present invention is a form such as storage of sulfonimide having a polymerizable functional group with improved stability against natural polymerization, while reducing halides, which were difficult to manufacture by the conventional method, and a method for preparing a sulfone imide solution, and a sulfone A method for removing halogen ions in an imide solution is provided. The present invention is an organic solvent solution of sulfonimide represented by the general formula (1), wherein the content of halogen ions relative to the amount of sulfonimide in the solution is 1000 ppm or less, a method for producing an organic solvent solution and a sulfonimide solution And a method of removing halogen ions in a sulfonimide solution.

Novel method for synthesis of (e)-stilbene derivatives, enabling to obtain resveratrol and piceatannol

FIELD: chemistry. SUBSTANCE: invention relates to versions of a novel method of producing a (E)-stilbene derivative of formula , used to produce polyhydroxystilbenes, particularly resveratrol or piceatannol, which exhibit antioxidant effect, novel intermediate compounds of formula , , and used in said methods, as well as use of the compound of formula , , (III), (IV) or (VII) as an intermediate compound in the synthesis of the (E)-stilbene derivative of formula (VI) or polyhydroxystilbene. Values of substitutes R 1 , R 1 ', R 2 ', R, A, Ar, R' are given in the claim. EFFECT: improved properties of the compound. 26 cl, 1 dwg, 32 ex РОССИЙСКАЯ ФЕДЕРАЦИЯ (19) RU (11) 2 443 671 (13) C2 (51) МПК C07C C07C C07C C07C C07C C07C ФЕДЕРАЛЬНАЯ СЛУЖБА C07D ПО ИНТЕЛЛЕКТУАЛЬНОЙ СОБСТВЕННОСТИ C07C C07C (12) ОПИСАНИЕ 43/215 41/09 41/18 69/738 49/255 243/42 321/00 45/65 67/343 (2006.01) (2006.01) (2006.01) (2006.01) (2006.01) (2006.01) (2006.01) (2006.01) (2006.01) ИЗОБРЕТЕНИЯ К ПАТЕНТУ (21)(22) Заявка: 2009107169/04, 25.07.2007 Приоритет(ы): (30) Конвенционный приоритет: 28.07.2006 FR 0653178 (73) Патентообладатель(и): КЛАРИАНТ СПЕШИАЛТИ ФАЙН КЕМИКАЛЗ (ФРЭНС) (FR) (43) Дата публикации заявки: 10.09.2010 Бюл. № 25 C 2 2 4 4 3 6 7 1 R U C 2 (56) Список документов, цитированных в отчете о поиске: A.Talvitie et al "Enrichment, Characterization and Absolute Configuration of the Enantiomers of 1-(3,5-Dimethoxyphenyl)-2-(4methoxyphenyl)ethanol". Acta Chemica Scandinavica, 1996, 50, 1143-1146. J.C.Roberts et al "The photochemistry of 1-(3,5dimethoxyphenyl)-2-(4-methoxyphenyl)ethyl ethanoate in alcohol solvents: A search for carbocation (см. прод.) (85) Дата начала рассмотрения заявки PCT на национальной фазе: 02.03.2009 (86) Заявка PCT: EP 2007/057650 (25.07.2007) (87) Публикация заявки РСТ: WO 2008/012321 (31.01.2008) Адрес для переписки: 129090, Москва, ул.Б.Спасская, 25, стр.3, ООО "Юридическая фирма Городисский и Партнеры", пат.пов. Е.Е. Назиной (54) НОВЫЙ СПОСОБ СИНТЕЗА (Е ...

Hydrazide derivatives

(E) -3-aryl-3- (2-methylhydrazino) propionate compound and preparation method and application thereof

本发明提供一种(E)‑3‑芳基‑3‑(2‑甲基肼基)丙酸酯类化合物及其制备方法。该方法以芳基酮与碳酸二酯为原料，在弱回流的条件下高收率地制备芳基β‑酮酸酯类化合物，接着与对甲基苯磺酰肼反应，高收率、高区域选择性地制备(E)‑3‑芳基‑3‑(2‑甲基肼基)丙酸酯类化合物。该制备方法以甲醇、乙醇等醇类为溶剂进行反应。本发明具有反应条件相对温和、操作简便、区域选择性高、收率高等特点，合成的(E)‑3‑芳基‑3‑(2‑甲基肼基)丙酸酯类化合物可用于制备吡唑啉类化合物。

Phenolic hydrazone macrophage migration inhibitory factor inhibitors

Provided are various compounds of Formula (I): Also provided are pharmaceutical compositions comprising the above compounds. Additionally, methods of inhibiting macrophage migration inhibitory factor (MIF) activity in a mammal are provided, as are methods of treating or preventing inflammation in a mammal. Further provided are methods of treating a mammal having sepsis, septicemia, and/or endotoxic shock. Also provided are methods of treating a mammal having an autoimmune disease, and methods of treating a mammal having a tumor.

Patent RU2018130292A3

`”ВУ“” 2018130292” АЗ Дата публикации: 12.03.2020 Форма № 18 ИЗ,ПМ-2011 Федеральная служба по интеллектуальной собственности Федеральное государственное бюджетное учреждение ж 5 «Федеральный институт промышленной собственности» (ФИПС) ОТЧЕТ О ПОИСКЕ 1. . ИДЕНТИФИКАЦИЯ ЗАЯВКИ Регистрационный номер Дата подачи 2018130292/04(048988) 22.01.2017 РСТ/СМ№2017/072078 22.01.2017 Приоритет установлен по дате: [ ] подачи заявки [ ] поступления дополнительных материалов от к ранее поданной заявке № [ ] приоритета по первоначальной заявке № из которой данная заявка выделена [ ] подачи первоначальной заявки № из которой данная заявка выделена [ ] подачи ранее поданной заявки № [Х] подачи первой(ых) заявки(ок) в государстве-участнике Парижской конвенции (31) Номер первой(ых) заявки(ок) (32) Дата подачи первой(ых) заявки(ок) (33) Код страны 1. 201610044990.8 22.01.2016 СМ Название изобретения (полезной модели): [Х] - как заявлено; [ ] - уточненное (см. Примечания) СПОСОБ ПРОИЗВОДСТВА ДЛИННОЦЕПОЧЕЧНОГО СПИРТА ЦИКЛОГЕКСЕНОНА ВЫСОКОЙ СТЕПЕНИ ОЧИСТКИ Заявитель: ТАЙХО ФАРМАСЬЮТИКАЛ КО. ЛТД., Р 2. ЕДИНСТВО ИЗОБРЕТЕНИЯ [Х] соблюдено [ ] не соблюдено. Пояснения: см. Примечания 3. ФОРМУЛА ИЗОБРЕТЕНИЯ: [Х] приняты во внимание все пункты (см. п см. Примечания [ ] приняты во внимание следующие пункты: [ ] принята во внимание измененная формула изобретения (см. Примечания) 4. КЛАССИФИКАЦИЯ ОБЪЕКТА ИЗОБРЕТЕНИЯ (ПОЛЕЗНОЙ МОДЕЛИ) (Указываются индексы МПК и индикатор текущей версии) С07С 45/42 (2006.01) С07С 49/713 (2006.01) С07С 251/84 (2006.01) С07С 249/16 (2006.01) С07С 49/753 (2006.01) С07С 311/49 (2006.01) 5. ОБЛАСТЬ ПОИСКА 5.1 Проверенный минимум документации РСТ (указывается индексами МПК) С07С 45/42, С07С 249/16, СО7С 49/713, С07С 49/753, СО7С 251/84, С07С 311/49 5.2 Другая проверенная документация в той мере, в какой она включена в поисковые подборки: 5.3 Электронные базы данных, использованные при поиске (название базы, и если, возможно, поисковые термины): РУ/РТ, ЕАРАТГУ, Ебрасепе, ...

Hydrazine derivatives

Hydrazine derivatives of formula (I) wherein Y signifies CO or SO2; R1 signifies lower alkyl, lower alkenyl, lower cycloalkyl, lower cycloalkyl-lower alkyl, aryl or aryl-lower alkyl; R2 signifies lower alkyl, halo-lower alkyl, aryl-lower alkyl, aryl-lower alkenyl or aryl when Y signifies SO2 and signifies lower alkyl, halo-lower alkyl, lower alkoxy, lower alkoxycarbonyl, acyl, lower cycloalkyl, aryl, aryl-lower alkyl, aryl-lower alkoxy or NR5R6 when Y signifies CO; and R3 signifies hydrogen, lower alkyl optionally substituted by cyano, amino, hydroxy, lower alkoxy, lower alkoxycarbonly, heterocyclyl or heterocyclylcarbonyl, lower alkenyl, lower alkynyl, lower cycloalkyl, lower cycloalkyl- lower alkyl, aryl-lower alkyl, aryl-lower alkenyl, aryl or heterocyclyl; or R2 and R3 together form the residue of a 5-, 6- or 7- membered cyclic amide, cyclic imide, cyclic sulphonamide or cyclic urethane group; R4 signifies lower alkyl, hydroxy-lower alkyl, lower alkenyl, lower cycloalkyl, lower cycloalkly-lower alkyl or a grouping of the formula Xaryl, X-heteroaryl or -(CH2)1-2-CH=CR7R8; X signifies a spacer group; R5 and R6 each individually signify hydrogen, lower alkyl or aryl-lower alkyl; and R7 and R8 together represent a lower alkylene group in which one methylene group is optionally replaced by a hetero atom; and their pharmaceutically acceptable salts inhibit not only the release of tumour necrosis factor (TNF-.alpha.) and transforming growth factor (TGF-.alpha.) from cells, but also keratinocyte proliferation. They are useful as medicaments, especially for the treatment of inflammation, fever, haemorrhage, sepsis, rheumatoid arthritis, osteoarthritis, multiple sclerosis or psoriasis.

Use of phenyl heterocycles in the relief or treatment of rheumatoid arthritis, osteoarthritis, fever, pain, headache or dysmenorrhea

The invention relates to use of compounds of formula (I): (see formula I) in the relief or treatment of rheumatoid arthritis, osteoarthritis, fever, pain, headache or dysmenorrhea.

NEW HYDRAZINE DERIVATIVES

Les dérivés d'hydrazine de formule (CF DESSIN DANS BOPI) dans laquelleY signifie CO ou SO2 ;R1 signifie un groupe alkyle inférieur, alcényle inférieur, cycloalkyle inférieur, cycloalkyl (inférieur) alkyle inférieur, aryle ou aryl-alkyle inférieur;R2 signifie alkyle inférieur, halogénoalkyle inférieur, aryl-alkyle inférieur, aryl-alcényle inférieur ou aryle lorsque Y signifie SO2 et signifie alkyle inférieur, halogénoalkyle inférieur, alcoxy inférieur, alcoxy(inférieur) carbonyle, acyle, cycloalkyle inférieur, aryle, aryl-alkyle inférieur, aryl-alcoxy inférieur ou NR5 R6 lorsque Y signifie CO; etR3 signifie un atome d'hydrogène, un groupe alkyle inférieur éventuellement substitué par un groupe cyano, amino, hydroxy, alcoxy inférieur, alcoxy (inférieur) carbonyle, hétérocyclyle ou hétérocyclylcarbonyle, alcényle inférieur, alcynyle inférieur, cycloalkyle inférieur, cycloalkyl (inférieur) -alkyle inférieur, aryl-alkyle inférieur, aryl-alcényle inférieur, aryle ou hétérocyclyle; ouR2 et R3 forment ensemble le résidu d'un groupe amide cyclique, imide cyclique, sulfonamide cyclique ou uréthane cyclique à 5, 6 ou 7 chaînons; R4 signifie un groupe alkyle inférieur, hydroxyalkyle inférieur, alcényle inférieur, cycloalkyle inférieur, cycloalkyl (inférieur) -alkyle inférieur ou un groupement de formule X-aryle, X-hétéroaryle ou - (CH2 ) 1-2 -CH=CR7 R8 ; , X signifie un groupe espaceur;R5 et R6 signifient chacun individuellement un atome d'hydrogène, un groupe alkyle inférieur ou aryl-alkyle inférieur; etR7 et R8 représentent ensemble un groupe alkylène inférieur dans lequel un groupe méthylène est éventuellement remplacé par un hétéroatome; et leurs sels pharmaceutiquement acceptables, inhibent non seulement la libération du facteur alpha de nécrose tumorale (TNF-alpha) et la libération du facteur de croissance transformant (TGF-alpha) des cellules, mais aussi la prolifération des kératinocytes. Ce sont des médicaments utiles, en particulier pour le traitement ...

Molecule with desinsection effectiveness, and with the relevant intermediate of these molecules, composition and method

本公开涉及以下领域：对节肢动物门、软体动物门和线虫动物门中的害虫具有杀虫效用的分子，制备此类分子的方法，用于此类方法的中间体，含有此类分子的组合物，以及使用此类分子和组合物对抗此类害虫的方法。这些分子和组合物可以用作例如杀螨剂、杀昆虫剂、杀疥虫剂、杀软体动物剂和杀线虫剂。本文件公开了具有下式(“式1”)的分子。

"hydrazine derivatives"

Patente de Invenção: <B>"DERIVADOS DE HIDRAZINA"<D>. Derivados hidrazina de fórmula (I) onde Y significa CO ou SO~ 2~; R^ 1^ significa alquila inferior, alquenila inferior, ciclo alquila inferior, ciclo alquil inferior alquila inferior, arila ou aril alquila inferior; R^ 2^ significa alquila inferior, halo alquila inferior, aril alquila inferior, aril alquenila inferior ou arila quando Y significa SO~ 2~e significa alquila inferior, halo alquila inferior, alcóxi inferior, alcóxi carbonila inferior, acila, ciclo alquila inferior, arila, aril alquila inferior, aril alcóxi inferior ou NR^ 5^R^ 6^quando Y significa CO; e R^ 3^ significa hidrogênio, alquila inferior opcionalmente substituída com ciano amino, hidróxi, alcóxi, inferior, alcóxi carbonila inferior, hetero ciclila ou hetero ciclil carbonila, alquenila inferior, alquinila inferior, ciclo alquila inferior, ciclo alquil inferior, aril alquila inferior, aril alquenila inferior, arila ou hetero ciclila; R^ 2^e R^ 3^ juntos formam o resíduo de um grupo uretano cíclico sulfonamida cíclica, imida cíclica ou amida cíclica de 5, 6 ou 7 membros; R^ 4^ significa alquila inferior, hidróxi alquila inferior, alquenila inferior, ciclo alquila inferior, ciclo alquil inferior alquila inferior ou um grupamento da fórmula X-arila, X-heteroarila ou (CH~ 2~ )~ 1-2~ - CH= CR^ 7^R^ 8^, X significa um grupo espaçador; R^ 5^ e R^ 6^ cada um individualmente, significa hidrogênio, alquila inferior ou aril alquila inferior; R^ 7^ e R^ 8^ juntos representam um grupo alquileno inferior onde um grupo metileno está opcionalmente susbtituído com um heteroátomo; e seus sais farmaceuticamente aceitáveis inibem não somente a liberação de fator de necrose de tumor (TNF-<244>) de células, mas também proliferação de ceratinócitos. Eles são úteis como medicamentos, especialmente para o tratamento de inflamação, febre, hemorragia, sepsia, artrite reumatóide, osteartrite, esclerose múltipla ou psoríase.

Fluoroallylsulfonyl azide monomers and polymers there from

본 발명은 플루오로중합체 내 관능성 단량체로서 유용한, CF 2 =CF-CF 2 -O-R f -SO 2 N 3 화학식(I) (R f 는 선택적으로 1개 이상의 에테르성 산소 원자를 포함하는 2가 (과)불소화기임)의 플루오로알릴설포닐 아지드 화합물[단량체(Az)], 이러한 플루오로알릴설포닐 아지드 화합물로부터 유도된 반복단위를 포함한 플루오로중합체, 이들의 제조 방법, 이들을 포함한 경화성 화합물, 및 이들의 가교 방법에 관한 것이다.

Aromatic carboxylic acid derivatives for treatment and prophylaxis of gastrointestinal diseases including colon cancers

Prodrug compounds which metabolize into 5-ASA or analogs thereof, and taurine or analogs thereof, in the colon site are disclosed. Pharmaceutical compositions including the compounds, and methods of treatment using the compounds, are also disclosed. Such compounds have utility for treating or preventing gastrointestinal disorders, including colon cancer, ulcerative colitis and Crohn's disease.

Manufacturing method for high-purity cyclohexenone long-chain alcohol

The present invention relates to a manufacturing method for a high-purity cyclohexenone long-chain alcohol compound represented by formula (I). The manufacturing method for the compound represented by formula (I) adopts a metal-induced Barbier reaction. The invention has the advantages of a short reaction path, high yield, and high product purity, and is suitable for scaling up industrially.

Use of inhibitors of cyclooxygenase in the treatment of neurodegenerative diseases

The present invention provides a method of treating a neurodegenerative disease and in particular Alzheimers disease which comprises administering to a human in need thereof a therapeutically effective amount of a non-steroid COX-II inhibitor. Although a wide range of COX-II inhibitors may be employed but it is preferred to employ compounds of the Formula I: ##STR1##

Sulfonylhydrazines and their use as antineoplastic agents and as antitrypanosomal agents

Sulfonylhydrazines of the formula RSO 2 N(CH 2 CH 2 X)N(SO 2 CH 3 ) 2 , wherein R is an alkyl or an aryl and X is a halogen or OSO 2 Y, wherein Y is an alkyl or an aryl. Such sulfonylhydrazines are useful in treating cancer. Methylating agents of the formula (a) R'SO 2 N(CH 3 )N(SO 2 CH 3 ) 2 , wherein R' is an alkyl or an aryl and (b) R"SO 2 N(CH 3 )N(CH 3 )SO 2 R", wherein R" is an alkyl or an aryl. Such methylating agents are useful as antitrypanosomal and anticancer agents.

Method for preparing high-purity cyclohexenone long-chain alcohol

Fluoroallylsulfonyl azide monomers and polymers there from

This invention pertains to fluoroallylsulfonyl azide compounds of formula: CF2=CF-CF2-O-Rf-SO2N3 formula (I) wherein Rf is a divalent (per)fluorinated group, optionally comprising one or more than one ethereal oxygen atom [monomer (Az)], which are useful as functional monomers in fluoropolymers, to the fluoropolymers which comprise recurring units derived from such fluoroallylsulfonyl azide compounds, to a process for their manufacture, to a curable compound comprising the same and to a method for crosslinking the same.

SUBSTITUTED HYDRAZONE AS AN INHIBITOR OF CYCLOOXYGENASE-2

Sulphonated Amino Acid Derivatives and Metalloproteinase Inhibitors Containing Them

Guanidine compounds and use thereof

The present invention relates to guanidine compounds for inhibiting mitochondrial oxidative phosphorylation (OXPHOS) and use thereof. More specifically, the present invention relates to a pharmaceutical composition for preventing or treating a OXPHOS-related disease, particularly cancer by inhibiting mitochondrial oxidative phosphorylation and reprogramming cellular metabolism.

Phenyl heterocycles as COX-2 inhibitors

The invention encompasses the novel compound of Formula I useful in the treatment of cyclooxygenase-2 mediated diseases. ##STR1## The invention also encompasses certain pharmaceutical compositions for treatment of cyclooxygenase-2 mediated diseases comprising compounds of Formula I.

Sulfonated amino acid derivatives and metalloproteinase inhibitors containing the same

하기 화학식 I 로 표현되는, 메탈로프로테이나제 저해 활성을 갖는 화합물, 그의 광학적 활성 이성질체, 이들의 약제학적 수용가능염 또는 이들의 수화물. A compound having metalloproteinase inhibitory activity, an optically active isomer thereof, a pharmaceutically acceptable salt thereof, or a hydrate thereof represented by the following formula (I): [화학식 I] [Formula I]

Novel trienoic retinoid compounds and methods

Novel trienoic retinoid compounds having activity for retinoic acid receptors and retinoid X receptors are provided. Also provided are pharmaceutical compositions incorporating such compounds and methods for their use. Compounds of the following formulae are provided: <IMG>

Process for producing allene compound

本发明属于有机合成化学领域，具体涉及联烯化合物的制备方法。本发明提供式I化合物，其消旋体、立体异构体、互变异构体的制备方法，包括： 将式III化合物或式IV化合物或式V化合物与式II化合物、及SiR 3 ‑CN在铜盐、1,10‑菲啰啉的存在下反应得到式I‑1化合物。

Α7 NICOTINE ACETYLCHOLINE RECEPTOR MODULATORS AND THEIR APPLICATION

1. Соединение формулы (I) или его соль:где Rвыбран из необязательно замещенного арила, необязательно замещенного бензила, необязательно замещенного гетероарила или необязательно замещенного гетероциклила;Rвыбран из водорода, C-Cалкила, F, Cl, CN, фенила или C-Cгалогеналкила;Rвыбран из водорода, C-Cалкила, F, Cl, CN или C-Cгалогеналкила; илиRи Rвместе образуют C-Cциклоалкил или C-Cциклоалкенил;Rвыбран из необязательно замещенного гетероарила, необязательно замещенного гетероциклила или необязательно замещенного арила;Rвыбран из водорода или C-Cалкила;R-Rнезависимо выбраны из галогена или водорода; иn равно 1-3,где, когда Rи Rпредставляют собой водород, и n равно 1, Rне является (1) фенилом или фенилом, замещенным циклогексилом, гетероциклилом, F или ОСН; или (2) необязательно замещенным гетероарилом.2. Соединение по п. 1 или его соль, где Rвыбран из необязательно замещенного бензила; необязательно замещенного арила; необязательно замещенного гетероарила; или необязательно замещенного гетероциклила.3. Соединение по п. 1, представленное формулой (Ia), или его соль:где Rвыбран из группы, включающей необязательно замещенный низший алкил, необязательно замещенный арил, необязательно замещенный арилокси, необязательно замещенный гетероарил, необязательно замещенный гетероциклил, -P=О(ОН)(NH), -С(О)NR'R', -NR'S(О)NR'R', -NR'-S(О)R', -NR'C(О)R', -S(О)-NR'R' и -NR'R' (где каждый R' независимо выбран из водорода, низшего алкила, С-Сциклоалкила, гетероциклила, гетероарила, -OH или NH), -S(О)R” (где R” представляет собой низший алкил или циклоалкил) и -S(О)R'" (где R'" представляет собой низший алкил или циклоалкил);каждый Rнезависимо представляет собой -Н циано, галоген, нитро, необязательно замещенный низший алкил, необязательно замещенный арил, необязательно замещенный арилокси, РОССИЙСКАЯ ФЕДЕРАЦИЯ (19) RU (11) (51) МПК C07C 311/37 (13) 2015 106 915 A (2006.01) ФЕДЕРАЛЬНАЯ СЛУЖБА ПО ИНТЕЛЛЕКТУАЛЬНОЙ ...

Phenylhydrazine insecticidal derivatives

Lipoic acid derivatives and their use in treatment of disease

This invention relates to the identification of a novel class of therapeutic agents which selectively target and kill tumor cells and certain other types of diseased cells, and to compositions comprising lipoic acid derivatives which poison the pyruvate dehydrogenase complex specifically in such cells. This invention also provides for methods of using therapeutically effective amounts of the lipoic acid derivatives for the treatment of cancer and other diseases. The lipoic acid derivatives described herein have a wide range of preventive and therapeutic applications.

Preparation method of high-purity cyclohexenone long-chain alcohol

本发明涉及一种式I表示的高纯度环己烯酮长链醇的制备方法，采用金属介导的Barbier反应制备式I化合物。本发明方法具有以下优点：路线短、收率高、产品纯度高，适合工业放大。

Onium salt, negative resist composition and resist pattern forming method

Sulfonyl semicarbazides

Abstract of the Disclosure Organic sulfonyl semicarbazides are prepared by reacting a salt of a sulfinic acid with azodicarbonamide in the presence of water. E.g., reaction of sodium p-toluene sulfinate with azodicarbonamide in water yields p-toluene sulfonyl semicarbazide, userul as a blowing agent.

Hydrazide derivatives

A compound represented by the following general formula (1) or a salt thereof or a hydrate of the foregoing is safe while exhibiting suitable physicochemical stability, and is useful as therapeutic or prophylactic agents for diseases associated with thrombus formation. wherein R 1a , R 1b , R 1c and R 1d each independently represent hydrogen, etc., R 2 represents optionally substituted phenyl, etc., R 3 represents optionally substituted C6-10 aryl, etc., Z 1 , Z 2 and Z 3 each independently represent hydrogen, etc., Z 4 represents hydrogen, etc. and X represents a single bond or -CO-, etc.

Resorcinol derivatives

Guanidine compounds and uses thereof

本発明は、ミトコンドリアの酸化的リン酸化（ＯＸＰＨＯＳ）を抑制するためのグアニジン化合物及びその用途に関する。より具体的には、本発明は、ミトコンドリアの酸化的リン酸化を抑制し、細胞の代謝を再プログラミングすることにより、ＯＸＰＨＯＳに関連する疾患、特に癌を予防又は治療するための薬学組成物に関する。【代表図】図３

Lipoic acid derivatives and their use in treatment of disease

This invention relates to the identification of a novel class of therapeutic agents which selectively target and kill tumor cells and certain other types of diseased cells, and to compositions comprising lipoic acid derivatives which poison the pyruvate dehydrogenase complex specifically in such cells. This invention also provides for methods of using therapeutically effective amounts of the lipoic acid derivatives for the treatment of cancer and other diseases. The lipoic acid derivatives described herein have a wide range of preventive and therapeutic applications.

Resorcinol derivatives

The present invention relates to certain resorcinol derivatives and their use as skin lightening agents.

Process for the production of isoureas

Method for efficiently introducing acetoxyl group into beta position of fatty amine and fatty alcohol

一种在脂肪胺和脂肪醇的β位高效引入乙酰氧基的方法，将式(Ⅱ)的反应底物加入溶剂溶解，加入环状二酰基过氧化物和过渡金属，在加热的条件下得到式(I)；所述式(I)、式(II)中的R 1 与R 2 包括氢、卤素、烷基、芳基中的任意一种，X为对氧、对甲基苯磺酰基氮的任意一种。本发明使用环状二酰基过氧化物与过渡金属配位进行碳氢活化反应，同时作为氧化剂和配体，反应过程中生成的副产物双羧酸可以回收作为再次合成环状二酰基过氧化物的原料，原子经济性高；可以通过调节环状二酰基过氧化物的取代来灵活调控反应活性，精准可调可控，合成方法简单，产率高，更好地达到环境友好和绿色化学的目标。

Aryl sulfonohydrazides

Compound of formula (I) wherein A is selected from (i), where R

Indan-1,3-dione and indan-1,2,3-trione derivatives, processes for the preparation of same and their application as therapeutic agents

Compounds of formula (I) used as therapeutic agents. R2 and R3 are independently H, C1-C4 alkoxy or OH and (A, B) = (oxygen, oxygen) in which case either R or R1 is OH, halogen, secondary amino or tertiary amine while the other denotes NHNHCONHR4 or R and R1 together form =N-NH-CX-NHR5, =N-NH-CX-N(phenyl)2, =N-NH-CX-NH-NH-R5, =N-NH-C(SCH3)=N-R6 or =N-N=C(SCH3)-NH-R6; or (A, B) = (N-OH, oxygen) in which case R and R1 together form =N-NH-CX-NHR5 or =N-NH-CX-N(phenyl)2; or (A, B) = (N-NH-CX-NHR5, oxygen) in which case R and R1 together form =N-NH-CX-NHR5; or (A, B) = (N-OH, N-OH) in which case R and R1 together form =N-NH-CX-NHR5 or =N-NH-CX-N(phenyl)2.

Phenyl heterocycles as cox-2 inhibitors

Compounds for treating proliferative disorders

Phenyl heterocycles as cox-2 inhibitors

The invention encompasses the novel compound of Formula I useful in the treatment of cyclooxygenase-2 mediated diseases, ##STR1## The invention also encompasses certain pharmaceutical compositions for treatment of cyclooxygenase-2 mediated diseases comprising compounds of Formula I.

Glucagon antagonist / adverse agent

(57)【要約】 中央のヒドラジドモチーフを含む非ペプチド化合物、およびその合成方法。この化合物は、グルカゴンペプチドホルモンと拮抗する用に作用する。