ГЕТЕРОЦИКЛИЧЕСКИЕ СОЕДИНЕНИЯ В КАЧЕСТВЕ АНТАГОНИСТОВ CCR2B

Изобретение относится к новым соединениям общей формулы (I) или к их фармацевтически приемлемым солям, обладающим CCR2B антагонистической активностью, и к фармацевтической композиции на их основе. ! , ! где Р представляет собой фенил, возможно замещенный 1 или 2 заместителями, независимо выбранными из галогена, С1-4алкила, циано, трифторметила, С1-4алкокси и трифторметилтио, a R2 имеет значения, указанные в формуле изобретения. 2 н. и 14 з.п. ф-лы.

СПИРОЦИКЛИЧЕСКИЕ НИТРИЛЫ В КАЧЕСТВЕ ИНГИБИТОРОВ ПРОТЕАЗЫ

Настоящее изобретение относится к спироциклическим нитрилам формулы (Iа):, где радикалы А, В, С, X, Y, R24, R25, R26 и R27 представлены в п.1 формулы изобретения, ингибирующим тиолпротеазы, в частности катепсины, способу их получения и их применению в качестве лекарственного средства для лечения заболеваний, которые прямо или косвенно провоцируются катепсинами. 10 н. и 2 з.п. ф-лы, 3 табл., 105 пр.

ПРОИЗВОДНЫЕ ГИДРАЗИНА ИЛИ ИХ СОЛИ, ФАРМАЦЕВТИЧЕСКОЕ СРЕДСТВО, АМИНОАЛКИЛГИДРАЗИНЫ ИЛИ ИХ СОЛИ

Использование: в медицине как обладающие свойством ингибировать действие фермента ВИЧ- протеазы и антивирусной активностью. Сущность изобретения: производные гидразина общей формулы 1: R1R2N - C(R3 R4) - C(R5R6 - N(R7)N(R8R9) , где R1 и R9 независимо друг от друга - водород, низший алканоил, фенил(низш.) алканоил, фенил(низш). алканоил, в котором остаток низшего алконоила замещен карбамоилом, морфолино(низш.) алканоил, тиоморфолино(низш.) алканоил, пиридил(низш.) алканоил, хинолил(низш.) алканоил, тетразолил(низш. ) алканоил, амино(низш. ) алканоил, замещенный у аминного азота N-морфолино- или N-тиоморфолинокарбон - ил, галоген(низш.) алканоил, содержащий до трех атомов галогена, 2-(N-морфолино(низш.) алкилкарбамоил)-низший алканоил, 2-(N-пиридил(низш. ) алкилкарбамоил)-низший алканоил, низший алкоксикарбонил, фенил(низш. ) алкоксикарбонил, тетрагидрофуранил(низш.) алкилксикарбонил, низший алкилсульфонил, N-пиридил(низш.) алкил-N-(низш.) алкилкарбамоил, или ацильный остаток аминокислоты ...

ПРОИЗВОДНЫЕ ГУАНИДИНА, СПОСОБ ИХ ПОЛУЧЕНИЯ И ФАРМАЦЕВТИЧЕСКАЯ КОМПОЗИЦИЯ, ОБЛАДАЮЩАЯ ГИПОГЛИКЕМИЧЕСКОЙ АКТИВНОСТЬЮ

Предложены производные гуанидина формулы I, представленной в описании, и их фармацевтически приемлемые соли, где R1 является необязательно замещенным фенилом, R2 является необязательно замещенным амином, R3 - H или (C1-C4) алкил, R4-H1(C1-C6) алкил, карбоциклическое кольцо с 3-7 атомами углерода и др. R5-H1, галоид, (C1-C4) алкил, (C1-C3 )алкокси, S(O)m R8 и др., предложен также способ их получения, а также фармацевтическая композиция, обладающая гипогликемической активностью. 3 с. и 11 з.п. ф-лы, 2 табл.

ЗАМЕЩЕННЫЕ ПИПЕРАЗИНЫ, (1,4)-ДИАЗЕПИНЫ И 2,5-ДИАЗАБИЦИКЛО(2,2,1)ГЕПТАНЫ В КАЧЕСТВЕ Н1-И/ИЛИ Н3-АНТАГОНИСТОВ ГИСТАМИНА ИЛИ ОБРАТНЫХ Н3-АНТАГОНИСТОВ ГИСТАМИНА

... 1. Соединение формулы (I) где R1 представляет собой водород, -С1-6алкил, -С1-6алкокси, -С3-8циклоалкил, -С1-6алкил-С3-8циклоалкил, арил, гетероциклил, гетероарил, -С1-6алкил-арил, -С1-6 алкил-гетероарил, -С1-6алкил-гетероциклил, -арил-арил, -арил-гетероарил, -арил-гетероциклил, -гетероарил-арил, -гетероарил-гетероарил, -гетероарил-гетероциклил, -гетероциклил-арил, -гетероциклил-гетероарил, -гетероциклил-гетероциклил, где R1 может быть возможно замещен одним или более чем одним заместителем, которые могут быть одинаковыми или разными и которые выбраны из группы, состоящей из галогена, гидрокси, COOR15, циано, -С1-6алкил-циано, нитро, оксо, трифторметила, трифторметокси, фторметокси, дифторметокси, С1-6алкила (возможно замещенного группой COOR15), С2-6алкенила (возможно замещенного группой COOR15), С2-6алкинила (возможно замещенного группой COOR15), С1-6алкокси (возможно замещенного группой COOR15), пентафторэтила, C1-6алкокси, С2-6алкенокси, арила, арилС1-6алкила, -СО-арила (возможно замещенного ...

ЗАМЕЩЕННЫЕ БЕНЗОИЛЦИКЛОГЕКСЕНОНЫ И ИХ ПРИМЕНЕНИЕ В КАЧЕСТВЕ ГЕРБИЦИДНОГО СРЕДСТВА

... 1. Соединения формулы (I) в которой Q представляет собой О (кислород) или S (серу), R1 представляет собой водород, галоген или соответственно, при необходимости, замещенный алкил, алкилтио или арил, R2 представляет собой водород, галоген или, при необходимости, замещенный алкил, или вместе с R1 представляет собой O (кислород) или алкандиил (алкилен), R3 представляет собой водород, нитро, циано, карбокси, карбамоил, тиокарбамоил, галоген или соответственно, при необходимости, замещенный алкил, алкокси, алкилтио, алкилсульфинил, алкилсульфонил, алкиламино, диалкиламино, диалкиламино-карбонил или диалкиламиносульфонил, R4 представляет собой водород, нитро, циано, карбокси, карбамоил, тиокарбамоил, галоген или соответственно, при необходимости, замещенный алкил, алкокси, алкилтио, алкилсульфинил, алкилсульфонил, алкиламино, диалкиламино, диалкиламино-карбонил или диалкиламиносульфонил, R5 представляет собой водород или соответственно, при необходимости, замещенный алкил, алкокси, алкилтио, ...

БЕНЗИЛЭФИРАМИНЫ, ПОЛЕЗНЫЕ КАК АНТАГОНИСТЫ CCR-5

... 1. Соединение общей формулы I его энантиомеры, диастереомеры, соли и сольваты, в которой Х представляет собой связь или кислород; m представляет собой 0, 1, 2, 3 или 4; n представляет собой 0, 1 или 2; R1 представляет собой необязательный заместитель, независимо выбираемый в каждом случае из галогена, алкила, галоалкила, нитро или -NR5R6; R2 представляет собой a) водород; или b) алкил, циклоалкил, алкенил, арил или гетероарил, любой из которых может быть, необязательно, замещен группой Y; Y представляет собой a) арил или гетероарил, каждый из которых может быть, необязательно, замещен одним или несколькими Z1, Z2, Z3; b) циклоалкил или гетероцикло, каждый из которых может быть, необязательно, замещен одним или несколькими Z1, Z2, Z3; c) -COOR7; d) -NR8R9; e) CHR10(OR11); f) -C(=O)-NR8R9; g) -NR12-(C=O)-NR8 R9; h) -CN; i) -C(=N-OR13); j) алкокси; R3 и R4 независимо выбирают из a)водорода; b) алкила, циклоалкила, (циклоалкил)алкила, арила, (арил)алкила, гетероцикло, (гетероцикло)алкила, гетероарила ...

НОВЫЕ СОЕДИНЕНИЯ И КОМПОЗИЦИИ В КАЧЕСТВЕ ИНГИБИТОРОВ КАТЕПСИНА

... 1. Соединение формулы I где X1 и X2 оба представляют метилен, или X1 представляет этилен и X2 представляет связь; R3 представляет -CR5=CHR6, -CR5(CR63)2 или -CR7=NR8, где R5 представляет водород и R6 представляет водород, или (C1-4)алкил, или R5 и R6 вместе с атомами, к которым присоединены R5 и R6, образуют (C3-12 )циклоалкенил, гетеро(C5-12)циклоалкенил, (C6-12)арил, гетеро(C6-12)арил, (C9-12)бициклоарил или гетеро(C8-12)бициклоарил и R7и R8вместе с атомами, к которым присоединены R7 и R8, образуют гетеро(C5-12)циклоалкенил, гетеро(C6-12)арил или гетеро(C8-12 )бициклоарил, где R3 необязательно замещен 1-5 радикалами, независимо выбранными из группы, состоящей из (C1-4)алкила, циано, галогена, галогензамещенного (C1-4 )алкила, нитро, -Х4NR9R9, -X4OR9, -X4SR9, -Х4С(О)NR9R9, -X4C(O)OR9, -X4S(О)R10, -X4S(О)2 R10 и -X4С(О)R10, где X4 представляет связь или (C1-2)алкилен, R9 в каждом случае независимо представляет водород, (C1-3 )алкил или галогензамещенный (C1-3)алкил, и R10 представляет ( ...

Способ получения производных феноксипропиламина или их солей

9-[(Substituierte Glycyl)amido]-6-demethyl-6-deoxytetracycline als antibiotische Mittel

Hemmer der retroviralen Protease

Inhibitoren retroviraler Proteasen

Renin inhibierende N-(2-Amino-2-oxoethyl)-butandiamid-Derivate

GUANIDINO PROTEIASE INHIBITOREN

METALLSALZE VON 1,1,5,5-TETRASUBSTITUIERTEN DITHIOBIURETVERBINDUNGEN, IHRE HERSTELLUNG UND VERWENDUNG

1-ACYL-1-PHENYL-HARNSTOFFE

PIPERIDINE COMPOUNDS

N-Cyclische und N,N'dicyclische Harnstoffe

Verfahren zur Herstellung von neuen Harnstoffderivaten

ACIDIC AMINO ACID DIAMIDE DERIVATIVE

Therapeutic N-(2-biphenylyl)guanidine derivatives

Benzenesulphonyl-ureas and process for preparing them

... 1,132,098. Sulphonyl ureas. FARBWERKE HOECHST A.G. 7 Dec., 1965 [8 Dec., 1964], No. 51890/65. Heading C2C. Novel benzenesulphonyl ureas of the formula wherein Z represents oxygen or sulphur, R is hydrogen, lower alkyl or phenyl lower alkyl, the word "lower" indicating a group of 1-4 carbon atoms, R1 represents (a) C 2-8 alkyl or alkenyl, (b) phenyl lower alkyl, (c) cyclohexyl lower alkyl, (d) an endoalkylene-cyclohexyl, endoalkylene-cyclohexenyl, endoalkylene-cyclohexylmethyl or endoalkylene cyclohexenylmethyl group containing 1 or 2 endoalkylene carbon atoms, (e) lower alkyl-cyclohexyl or lower alkoxy-cyclohexyl, (f) C 5-8 cycloalkyl or (g) cyclohexenyl or cyclohexenyl-methyl, Y is a hydrocarbon chain of 1-4 carbon atoms and X and X1 represent hydrogen or a C 1-6 aliphatic hydrocarbon, C 5-8 cycloalkyl, cyclohexyl lower alkyl, lower alkyl cyclohexyl, phenyl or phenyl lower alkyl radical (wherein the phenyl ring may bear one or more lower alkyl, lower alkoxy, halogen, ...

Improvements relating to the preparation of new 1,4-unsymmetrically substituted piperazines

The invention comprises 1,4-unsymmetrically substituted piperazines having the general formula wherein O=C-R is an acyl radical, R being an alkyl, aryl or halo-aryl radical, such as for example, benzoyl, dichlorobenzoyl, o-chlorobenzoyl, acetyl, propionyl or n-butyryl. Such compounds are obtained by treating 1-carbamyl - 4 - carbobenzoxy - piperazine with hydrogen and a reducing agent and then reacting the 1-carbamyl-piperazine thus produced with an acylating agent, i.e. an acyl halide or acyl anhydride. The reduction can be effected by the action of hydrogen and a palladiumcharcoal catalyst, preferably in a neutral or weakly acidic medium such as water, ethanol or acetic acid. In Example (1) 1-carbamylpiperazine (from the reduction of 1-carbamyl-4-carbobenzoxy-piperazine) is reacted with benzoyl chloride to give 1-benzoyl-4-carbamylpiperazine. In a generally similar manner are prepared 1 - acyl - 4 - carbamyl - piperazines in which the acyl groups are respectively ...

Novel compounds

PHARMACEUTICAL COMPOSITIONS CONTAINING SUBSTITUTED BIRUETS COMPOUND

New aminoguanidine derivatives and a process for the preparation thereof

The invention relates to new aminoguanidine derivatives of the general formula (I), I wherein R1, R2 and R3 each represent hydrogen or halogen atom, C1-4 alkyl, nitro, trifluoromethyl or C1-4 alkoxy group, R4 and R5 represent a C1-4 alkyl group, furthermore NR4R5 may form a 5 to 7 membered saturated heterocyclic group containing either one or two nitrogen atoms or a nitrogen and an oxygen atom and being optionally substituted by one or two methyl, hydroxymethyl or hydroxyethyl groups, R6 and R7 each represent a hydrogen atom, normal or branched C1-4 alkyl or C2-4 alkenyl group, and to their pharmaceutically acceptable acid addition salts as well as to a process for the preparation thereof. The new compounds of the invention possess valuable antiarrhythmic activity and are devoid of the undesired circulatory side effects of the known antiarrhythmic compounds.

DIAZ(EP)INE BIS(N-AMIDINOAMIDINE)DERIVATIVES

PROCESS FOR OBTAINING NON-VOLATILE, LOW MOLECULAR WEIGHT MONO- AND POLYISOCYANATES CONTAINING TERTIARY AMINO GROUPS

... 1,205,486. Isocyanates containing tertiary amino groups. FARBENFABRIKEN BAYER A.G. 26 March, 1968 [29 March, 1967], No. 14484/68. Heading C2C. A process for the preparation of non-volatile, low molecular weight (of up to 1000) mono- and poly-isocyanates which contain tertiary amino groups, comprises reacting tertiary amines which contain one or more hydroxyl groups and/or one or more secondary and/or 1 to 3 primary amino groups with an aliphatic, cycloaliphatic or araliphatic diisocyanate, in which preferably at least 3 moles of said diisocyanate are used per mole of hydroxyl or amino groups which will react with an isocyanate, the reaction temperature preferably being between 20‹ and 120‹ C., and in which the unreacted diisocyanate is subsequently removed by continuous flow distillation or thin layer distillation under reduced pressure, at a temperature preferably between 80‹ and 200‹ C. The preparation of and 1 - methyl - 4 - (61 - isocyanate hexamethyleneamido)-piperazine is exemplified ...

Use of 2-Amino-Heterocycles

THERAPEUTIC AMIDINE DERIVATIVES METHOD OF REMOVING NITROGEN OXIDES AND SULPHUR TRIOXIDE FROM EXHAUST GASES

... 1455808 Adamantyl amidines and guanidines UPJOHN CO 5 Feb 1975 [11 Feb 1974] 4847/75 Heading C2C Novel compounds of Formula I wherein R 1 is adamantyl and R 2 is adamantyl, H, C 1-8 alkyl, C 5-8 cycloalkyl, phenyl(C 1-3 )alkyl or phenyl optionally substituted by C 1-3 alkyl, C 1-3 alkoxy, halogen or CF 3 , either R 3 and R 4 are each H, C 1-8 alkyl or C 5-8 cycloalkyl or NR 3 R 4 is pyrrolidino, piperidino, perhydroazepine, piperazino, C 1-3 alkyl piperazino, morpholino or thiumorpholino and pharmaceutically acceptable salts thereof, are prepared either by reaction of HNR3R4 with a compound or a compound R 1 NHCSNHR2 with phosgene or triphenylphosphine. N - 1 - Adamantyl - N1 - cyclohexylthiourea is obtained from 1-adamantyl isothiocyanate, N - 1 - adamantyl - 4 - morpholinethiocarboxamide is obtained from 1-adamantane isothiocyanate and morpholine and N,N1-di-2-adamantylthiourea is obtained by reacting 2-adamantylamine with 1,11-thiocarbonyldiimidazole ...

Cardiac stimulants

The derivatives having the formula:- wherein R<3> and R<4>, which may be the same or different, are each hydrogen, or hydroxy (at least one being OH), R is hydrogen, methyl or ethyl and R<2> is methyl, ethyl or -CH2CH2OR; or R and R<2> together form an ethylene (-CH2CH2-) radical and their acid- addition salts, possess cardioselective beta adrenergic stimulant activity.

Thiourea derivatives

A new class of thiourea derivatives of the formula, wherein R1, and R2, which may be the same or different, are hydrogen, C1-C4 alkyl, C3-C5 alkenyl, benzyl, phenyl, adamantyl or tricycloundecyl, provided that when either R1 and R2 is adamantyl or tricycloundecyl, then the other is hydrogen or one of aforesaid groups other than adamantyl and tricycloundecyl, or R1 and R2, together with the adjacent nitrogen atom, form piperidene or pyrrolidene, each of which may be substituted with hydroxy, which are useful as antiviral agents, are prepared by reacting 3- isothiocyanate-4-homoisotwistane with a compound of the formula, wherein R1 and R2 are as defined above.

PROCESS OF PREPARING SILVER HALIDE PHOTOGRAPHIC EMULSION

Formamidine sulphite and disulphides and thiocarbamoyl guanidines having herbicidal activity, their preparation and use

A method of combatting weeds comprising applying to the soil pre- emergence and/or post-emergence of said weeds at a dosage rate of from 1 to 6 kg/ha one or more herbicide compounds having the general formula in which: each R represents a phenyl group which may be substituted by one or more substituents selected from halogen atoms, an alkyl group having one to three carbon atoms and a haloalkyl group having 1 to 3 carbon atoms, R<1> and R<2> independently represent an alkyl group having 1 to 3 carbon atoms, and alkoxyl group having 1 to 3 carbon atoms or R<1> and R<2> together form an alkylidenic chain of 4 or 5 carbon atoms which may be interrupted by a heteroatom, and n is 1 or 2. Many of the compounds of formulae (I) and (II) are new. The compounds may be prepared by the following reactions: ...

Vinyl sulfides of substituted ureas and thioureas and polymers and copolymers thereof

The invention comprises polymers and copolymers of compounds of the following formulae:-I: CH2=CH,S,#j(NHCX)nNR1R2; II: CH2=CH,S,A,NR3,CX,NR1R2; III:(CH2=CH.S.#j.NH.CX.NH)mR4; IV: (CH2=CH,S,A,NR3,CX,NH)mR4, where A is C2-C6 alkylene, #j is o- or p-phenylene optionally mono- or disubstituted by C1-C4 alkyl, R1 is H, C1-C18 alkyl, alkenyl, cycloalkyl, aralkyl, aryl or chloroaryl, R2 is H, methyl or ethyl (or NR1R2 is a morpholino, piperidino or pyrrolidino residue), R3 is H or C1-C4 alkyl, R4 is C4-C10 alkylene, phenylene, tolylene, methylene-bis-phenylene, methylidyne-tris-phenylene or dias nisylene, X is O or S, m is 2 or 3, and n is 1, or is 2 if R1=R2=H and X=O. Polymerization can be effected in bulk, solution, emulsion or suspension using as catalysts organic peroxides, azo compounds, boron trifluoride, sulphur dioxide, stannic chloride or aluminium chloride. The compounds may be copolymerised with acrylic and methacrylic acids, esters, amides and nitriles; esters of maleic, fumaric, ...

Benzènesulfonyl-semicarbazides and their preparation.

Azabicyclic carbamoyloxy mutilin derivatives for antibacterial use.

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

Carbamoyloxy derivatives of mutiline and their use as antibacterials.

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

Novel compounds

Guanidinobenzamides as MC4-R agonists

Compounds of formula (IA) and (IB) arc new where the variables R1 through R10 have the values set forth herein. Such compounds have use in treating diseases such as obesity and type Tl diabetes, and may be provided as pharmaceutical formulations in conjunction with a pliarmaceutically acceptable carrier- ...

Proatease inhibitors.

The present invention provides compounds which inhibit proteases, including cathepsin k, pharmaceutical compositions of such compounds, and methods for treating diseases of excessive bone loss or cartilage or matrix degradation, including osteoporosis; gingival disease including gingivitis and periodontitis; arthritis, more specifically, osteoarthritis and rheumatoid arthritis; paget's disease; hypercalcemia of malignancy; and metabolic bone disease, comprising inhibiting said bone loss or excessive cartilage or matrix degradation by administering to a patient in need thereof a compound of the present invention.

NOVEL PIPERAZINE

A compound of formula (1)or the pharmaceutically acceptable salt thereof; wherein a,b,c,d,e,j,R1,R2,R3, and R4, are as defined above useful to treat inflammation and other immune disorders.

Novel compounds.

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

Method of preparation of new cyclic urea derivatives and their salts.

Carbamoyloxy derivatives of mutiline and their useas antibacterials.

Method of preparation of derived from urea usable in particular to fight against bad grasses.

Novel piperazine derivatives.

1,4-Diamino-2,3-Dihydroxybutanes.

Method of inhibiting cathepsin k

New para-subtituted 3-phenoxy-1-carbonylaminoalkylaminopropanol-2-S having beta receptor blocking properties.

Protease inhibitors

New agents biocides.

New derivatives of the xanthine, their methods of preparation and the compositions pharmaceutical containing them.

Guanidinobenzamides as mc4-r agonists

Novel piperazine derivatives

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

Guanidinobenzamides as mc4-r agonists

Novel compounds

Novel compounds

Novel piperazine derivatives

PROCEDURE AND INTERMEDIATE FOR THE PRODUCTION OF RETROVIRALEN PROTEASEHEMMERN

GUANIDINOBENZAMIDE AS MC4-R AGONISTEN

PROCEDURE FOR THE PRODUCTION OF A NEW ALKANOL OF AMINE DERIVATIVE

Use and process for the preparation of N-cyclic and N,N'- dicyclic ureas

The use of ureas in which at least one of the two nitrogen atoms of the urea is part of a nonaromatic ring which can be interrupted by an oxygen or sulphur atom as chemical solvent, and a process for the preparation of tri- or tetralkylated ureas or diureas, wherein at least one of the nitrogen atoms of the urea is part of a nonaromatic ring which can be interrupted by an oxygen or sulphur atom, by dialkylation of the -NH2 group of a urea with an alkylene or alkylenearylenealkylene dihalide, disulphonate or dihydrogensulphate in the presence of a solid base and of a phase transfer catalyst.

PROCEDURE FOR THE PRODUCTION OF NEW CARBAMOYLAMINOALKYLBENZOLSULFONYLHARNSTOFFEN AND THEIR SALTS

PROCEDURE FOR the PRODUCTION OF 11 (1 - PIPERAZINYL) DIBENZO (B, F) (1,4) - THIAZEPIN, an INTERMEDIATE PRODUCT IN the SYNTHESIS of the ANTIPSYCHOTI DRUG QUETIAPIN

VERFAHREN ZUR HERSTELLUNG VON NEUEN DIPHENYLBUTYL-PIPERAZINCARBOXAMIDEN UND DEREN SAEURE- ADDITIONSSALZEN

VERFAHREN ZUR HERSTELLUNG VON NEUEN 3-(P-UREIDOPHENOXY)-2-HYDROXY-AMINOPROPANEN SOWIE DEREN SAUREADDITIONSSALZEN

VERFAHREN ZUR HERSTELLUNG VON NEUEN ACYLAMINOALKYLBENZOLSULFONYLSEMICARBAZIDEN UND DEREN SALZEN

MUTILINDERIVATE AND YOUR USE AS DRUGS

ALPHA SULFONYLAMINO ACETONITRILE ONE

NITRILES USABLE AS REVERSIBLE CYSTEIN PROTEASE INHIBITORS

VERFAHREN ZUR HERSTELLUNG NEUER SUBSTITUIERTER AMINOGUANIDIN-DERIVATE

VERFAHREN ZUR HERSTELLUNG VON NEUEN OXALYLHARN- STOFFEN

PROCEDURE FOR the PRODUCTION OF NEW ONE 3 (P-UREIDOPHENOXY) - 2-HYDROXY-AMINOPROPANEN AS WELL AS THEIR SOUR ADDITION SALTS

PROCEDURE FOR the PRODUCTION OF NEW ONE 3 (P-UREIDOPHENOXY) - 2-HYDROXY-AMINOPROPANEN AS WELL AS THEIR SOUR ADDITION SALTS

INSECTICIDE OR AKARIZIDES MEANS

PROCEDURE FOR THE PRODUCTION OF NEW DIPHENYLBUTYL DIPHENYLBUTYLPIPERAZINCARBOXAMIDE ONE AND - CARBOTHIOAMIDEN AND THEIR SAEUREADDITIONSSALZEN

USE AND PROCEDURE FOR the PRODUCTION OF N-CYCLI AND N, N' DICYCLI UREA

INHIBITORS THAT RETROVIRALEN PROTEASE

SUBSTITUTED UREA, YOUR PRODUCTION AND USE AS HERBICIDES AND MEANS FOR IT.

NEW THIOHYDRAZIN-1,2-DICARBONSAEURE-DERIVATE, PROCEDURE FOR YOUR PRODUCTION AND YOUR USE.

ARYLOXYHARNSTOFFE, THEIR PRODUCTION AND USE.

GUANIDINDERIVATE WITH THERAPEUTIC EFFECT

UREA-SUBSTITUTED BENZOYLGUANIDINE, PROCEDURE FOR YOUR PRODUCTION, YOUR USE AS MEDICINE OR DIAGNOSTIKUM AS WELL AS IT CONTAINING MEDICINE

HYDRAZONE OF INDANTRIONE AND YOUR THERAPEUTIC USE

ECYL UREA

MORPHOLINOHARNSTOFF DERIVATIVES

ENDOPARASITIZIDE MEANS ON BASIS OF DIDEPSIPEPTIDEN, NEW ONE DIDEPSIPEPTIDE AND PROCEDURE FOR YOUR PRODUCTION

N-CYANOMETHYLAMIDE ONE AS PROTEASE INHIBITORS

Procedure for the production of new Dibenz [b, f] [1,4] - oxazepinen and their acid addition salts

ASPARAGINE ACID DERIVATIVES, YOUR PRODUCTION AND USE

Procedure for the production of new hetero-cyclic connections and their salts

Fungicide means

Procedures for the production of new Pyrrolidin N CARBONIC ACID halogenaniliden

Procedure for the production of new Dibenz [b, f] [1,4] oxazepinen and their acid addition salts

Procedure for the production of new Dibenz [b, f] [1,4] oxazepinen and their acid addition salts

HEXENONE COMPOUNDS AND MEDICAL USE THEREOF

The present invention relates to a compound of Formula I, or an isomer, pharmaceutically acceptable salt and solvate thereof; to a composition comprising a compound of Formula I, or an isomer, pharmaceutically acceptable salt and solvate thereof, and a pharmaceutically acceptable carrier, excipient or diluent; and also to use of a compound of Formula I, or an isomer, pharmaceutically acceptable salt and solvate thereof for combating apoptosis, or preventing or treating a disease or disorder associated with apoptosis; and especially use for protecting cardiomyocyte, or preventing or treating a disease or disorder associated with cardiomyocyte apoptosis. 4. The compound according to having the following structure claim 1 , or its isomers claim 1 , pharmaceutically acceptable salts and solvates:(1) (1E)-1-phenyl-5-(1-morpholinylthiocarboxamido)-6,6,6-trichloro-1-ene-3-hexanone.5. A pharmaceutical composition comprising a compound or an isomer claim 1 , pharmaceutically acceptable salt and solvate thereof according to claim 1 , and a pharmaceutically acceptable carrier claim 1 , excipient or diluent.6. Use of the compound or an isomer claim 1 , pharmaceutically acceptable salt and solvate thereof according to in manufacture of a medicament for combating apoptosis claim 1 , or preventing or treating a disease or disorder associated with apoptosis.7. Use of the compound or an isomer claim 1 , pharmaceutically acceptable salt and solvate thereof according to in manufacture of a medicament for protecting cardiomyocyte claim 1 , or preventing or treating a disease or disorder associated with cardiomyocyte apoptosis.8. A method for combating apoptosis claim 1 , or preventing or treating a disease or disorder associated with apoptosis comprising administering a subject in such need a therapeutically effective amount of a compound or an isomer claim 1 , pharmaceutically acceptable salt and solvate thereof according to .9. A method for protecting cardiomyocyte claim 1 , or ...

Protease Activated Receptor 2 (PAR2) Antagonists

A compound of formula (I) or a pharmaceutically acceptable salt, solvate, or hydrate thereof 2. A compound according to wherein Rand Rare independently selected from H claim 1 , Calkyl claim 1 , or cyclopropyl claim 1 , each of which Calkyl claim 1 , or cyclopropyl being optionally substituted with one or more substituents independently selected from fluoro and Calkoxy4. A compound according to wherein the ring comprising Z and Y is optionally substituted with one more substituents independently selected from fluoro claim 1 , C-alkyl claim 1 , C-alkoxy claim 1 , fluoro-C-alkyl and fluoro-C-alkoxy.7. A compound according to any wherein Ris hydrogen.8. A compound according to wherein W is an optionally substituted phenyl ring.9. A compound according to wherein the Rsubstituent is optionally substituted with one or more fluoro substituents10. A compound according to wherein Ris H.11. A compound according to wherein Ris H or methyl.12. A compound according to wherein Ris H or methyl.14. (canceled)15. A compound according to wherein U═O.16. A compound according to wherein X is independently selected from —C(O)— claim 1 , —(CHR)— claim 1 , —N(R)— or claim 1 , in either orientation claim 1 , —(CHCHR)—.17. A compound according to wherein Q is independently selected from —O— claim 1 , —S— claim 1 , —N(R)— claim 1 , —C(O)— claim 1 , C(H)(OH)— claim 1 , —(CHR)— or claim 1 , in either orientation claim 1 , —(CHCHR)—.18. A compound according to wherein X is independently selected from —C(O)— claim 1 , —(CHR)— claim 1 , or —N(R).19. A compound according to wherein Q is independently selected from —O— claim 1 , —N(R)— claim 1 , —C(O)— claim 1 , C(H)OH)— claim 1 , —(CHR)—.20. A compound as claimed in selected from:(4-{[(4-Benzylpiperidin-1-yl)carbonylamino]methyl}phenyl)methanaminium chloride;2,2,2-Trifluoroacetic acid; N-{[4-(aminomethyl)phenyl]methyl}-4-[(4-methoxyphenyl)methyl]piperidine-1-carboxamide:2,2,2-Trifluoroacetic acid; N-{[4-(aminomethyl)phenyl]methyl}-4-[(3- ...

Opsin-Binding Ligands, Compositions and Methods of Use

Compounds and compositions of said compounds along with methods of use of compounds are disclosed for treating ophthalmic conditions related to mislocalization of opsin proteins, the misfolding of mutant opsin proteins and the production of toxic visual cycle products that accumulate in the eye. Compounds and compositions useful in the these methods, either alone or in combination with other therapeutic agents, are also described. 3. The compound of claim 2 , wherein Rand Rare each independently hydrogen or methyl.4. The compound of claim 2 , wherein Rand Rare each independently hydrogen or lower alkyl.6. The compound of claim 5 , wherein a and b are each 1 claim 5 , X is hydrogen claim 5 , Y is C—C(O)NRRor N—C(O)NRRwherein R claim 5 , Rand Rare all hydrogen.7. The compound of claim 1 , wherein X is H claim 1 , lower alkyl or —C≡CR.8. The compound of claim 1 , wherein Y is O or N—C(O)—NRR.920-. (canceled)21. A method of reducing or inhibiting mislocalization of an opsin protein claim 1 , comprising contacting an opsin protein with a compound of .22. The method of claim 21 , wherein said opsin protein is pressent in a rod cell or a cone cell.23. (canceled)24. The method of claim 22 , wherein said cell is present in a mammalian eye.25. A method of inhibiting the formation or accumulation of a visual cycle product claim 1 , comprising contacting an opsin protein with a compound of .26. The method of claim 25 , wherein said visual cycle product is lipofuscin or N-retinylidene-N-retinylethanolamine (A2E).27. A method of treating or preventing an ophthalmic condition in a subject at risk thereof claim 1 , comprising administering to the subject an effective amount of a compound of .28. The method of claim 27 , wherein said ophthalmic condition is an ocular protein mislocalization disorder.29. The method of claim 27 , wherein said ophthalmic condition is selected from the group consisting of wet or dry age related macular degeneration (ARMD) claim 27 , retinitis pigmentosa ...

MEDICAMENTS FOR THE TREATMENT OR PREVENTION OF FIBROTIC DEISEASES

The present invention relates to the use of indolinones of general formula 1. A method for treating fibrosis in rheumatoid arthritis , comprising administering to patient in need thereof a therapeutically effective amount of 3-Z-[1-(4-(N-((4-methyl-piperazin-1-yl)-methylcarbonyl)-N-methyl-amino)-anilino)-1-phenyl-methylene]-6-methoxycarbonyl-2-indolinone , or a salt thereof.2. The method of wherein 3-Z-[1-(4-(N-((4-methyl-piperazin-1-yl)-methylcarbonyl)-N-methyl-amino)-anilino)-1-phenyl-methylene]-6-methoxycarbonyl-2-indolinone is in the form of a monoethanesulfonate salt.3. The method of further comprising administering an additional pharmacologically active substance selected from the group consisting of anticholinergic agents claim 1 , beta-2 mimetics claim 1 , steroids claim 1 , PDE-IV inhibitors claim 1 , p38 MAP kinase inhibitors claim 1 , NK1 antagonists claim 1 , LTD4 antagonists claim 1 , EGFR inhibitors and endothelin-antagonists.4. The method of claim 3 , wherein the 3-Z-[1-(4-(N-((4-methyl-piperazin-1-yl)-methylcarbonyl)-N-methyl-amino)-anilino)-1-phenyl-methylene]-6-methoxycarbonyl-2-indolinone claim 3 , or salt thereof claim 3 , and the additional pharmacologically active substance together comprise a pharmaceutical composition that further comprises one or more pharmaceutically acceptable carriers or excipients. The present invention relates to a new use of indolinones of general formulasubstituted in the 6 position, the tautomers, the diastereomers, the enantiomers, the mixtures thereof and the salts thereof, particularly the physiologically acceptable salts thereof.Compounds of the above general formula I, the tautomers, the diastereomers, the enantiomers, the mixtures thereof and the salts thereof, particularly the physiologically acceptable salts thereof, have been described in WO 01/27081 and WO 04/13099 as having valuable pharmacological properties, in particular an inhibiting effect on various kinases, especially receptor tyrosine kinases such ...

Biguanide compound and use thereof

The present invention relates to a guanidine compound and a use thereof, and more specifically, to a guanidine derivative showing excellent effects of inhibiting cancer cell proliferation, cancer metastasis, and cancer recurrence; a preparation method thereof; and a pharmaceutical composition containing the same as an active ingredient. Compared to existing drugs, the guanidine derivative according to the present invention shows excellent effects of inhibiting cancer cell proliferation, cancer metastasis, and cancer recurrence even with small doses, and may thus be effectively used in preventing or treating various cancers such as uterine cancer, breast cancer, stomach cancer, brain cancer, rectal cancer, colorectal cancer, lung cancer, skin cancer, blood cancer, liver cancer, etc., inhibiting cancer cell proliferation and cancer metastasis.

N1-Cyclic Amine-N5-Substituted Biguanide Derivatives, Methods of Preparing the Same and Pharmaceutical Composition Comprising the Same

A N1-cyclic amine-N5-substituted biguanide derivative of Formula 1 or a pharmaceutically acceptable salt thereof, a method of manufacturing the same, and a pharmaceutical composition including the biguanide derivative or the pharmaceutically acceptable salt thereof as an active ingredient are provided. The biguanide derivatives have an effect of inhibiting cancer cell proliferation and also exhibit anticancer activity including inhibition of cancer metastasis and cancer recurrence, because they are effective in activating AMPK, which is associated with the control of energy metabolism, even when administered in a small dose compared with conventional drugs. Also, the biguanide derivatives are highly effective at lowering blood glucose and lipid concentration by AMPK activation, thus they may be effectively used to treat diabetes mellitus, obesity, hyperlipemia, hypercholesterolemia, fatty liver, coronary artery disease, osteoporosis, polycystic ovary syndrome and metabolic syndrome. 2. The compound of Formula 1 or the pharmaceutically acceptable salt thereof of claim 1 ,{'sub': 1', '2, 'wherein Rand Rare taken together with nitrogen to which they are attached to form 4- to 7-membered heterocycloalkyl,'}{'sub': 3', '3-7', '1-12', '3-12', '3-12, 'Ris Ccycloalkyl; or Calkyl unsubstituted or substituted with Caryl or Cheteroaryl,'}{'sub': 3-7', '3-12', '3-12', '1-4', '1-4, 'wherein Ccycloalkyl, 4- to 7-membered heterocycloalkyl, Caryl or Cheteroaryl is unsubstituted or substituted with at least one non-hydrogen substituent selected from the group consisting of halogen, Calkyl and Calkoxy, and the non-hydrogen substituent is unsubstituted or further substituted with halogen.'}3. The compound of Formula 1 or the pharmaceutically acceptable salt thereof of claim 1 ,{'sub': '3-12', 'wherein Caryl is a phenyl or naphthalenyl,'}{'sub': '3-12', 'Cheteroaryl is a furanyl, thiophenyl, pyridinyl, pyrrolyl, imidazolyl or pyrimidinyl,'}{'sub': 3-12', '3-12', '1-4', '1-4, 'Caryl or ...

COMPOSITIONS AND METHODS FOR INHIBITING GROUP II INTRON RNA

The present invention provides compositions and methods for inhibiting group II intron splicing for treating or preventing a disease or disorder associated with an organism harboring an active group II intron. The present invention also provides compositions and methods for inhibiting group II intron splicing for inhibiting, preventing or reducing growth of an organism harboring an active group II intron. 13-. (canceled)7. The compound of claim 4 , wherein R claim 4 , R claim 4 , and Rare OH.9. The compound of claim 4 , wherein Ris —C(═O)NHR.12. The compound of claim 11 , wherein R claim 11 , R claim 11 , and Rare OH.15. A method of reducing claim 11 , minimizing claim 11 , or preventing growth of an organism harboring an active group II intron claim 11 , the method comprising contacting the organism with an effective amount of an inhibitor of group II intron splicing.16. The method of claim 15 , wherein the inhibitor of group II intron splicing is at least one selected from the group consisting of a protein claim 15 , a peptide claim 15 , a peptidomimetic claim 15 , an antibody claim 15 , a ribozyme claim 15 , a small molecule chemical compound claim 15 , a nucleic acid claim 15 , an aptamer claim 15 , a modified nucleic acid claim 15 , a vector claim 15 , and an antisense nucleic acid molecule.17. (canceled)19. (canceled)20. A method of treating or ameliorating a disease associated with an organism harboring an active group II intron in a subject claim 15 , the method comprising administering an effective amount of a composition comprising an inhibitor of group II intron splicing to the subject.21. The method of claim 20 , wherein the disease or disorder is selected from the group consisting of a bacterial infection claim 20 , a yeast infection claim 20 , a fungal infection claim 20 , and a parasite infection.22. The method of claim 20 , wherein the subject is a mammal.23. The method of claim 22 , wherein the mammal is a human.24. The method of claim 20 , wherein ...

MEDICAMENTS FOR THE TREATMENT OR PREVENTION OF FIBROTIC DISEASES

The present invention relates to the use of indolinones of general formula 2. The method as recited in wherein the substituent in the 6 position of the substituted indolinone of formula I comprises a substituted amido group.3. The method as recited in wherein the indolinone of formula I is selected from the group consisting of:(a) 3-Z-[1-(4-(piperidin-1-yl-methyl)-anilino)-1-phenyl-methylene]-6-ethoxycarbonyl-2-indolinone,(b) 3-Z-[(1-(4-(piperidin-1-yl-methyl)-anilino)-1-phenyl-methylene]-6-carbamoyl-2-indolinone,(c) 3-Z-[1-(4-(piperidin-1-yl-methyl)-anilino)-1-phenyl-methylene]-6-methoxycarbonyl-2-indolinone,(d) 3-Z-[1-(4-(dimethylaminomethyl)-anilino)-1-phenyl-methylene]-6-ethoxycarbonyl-2-indolinone,(e) 3-Z-[1-(4-((2,6-dimethyl-piperidin-1-yl)-methyl)-anilino)-1-phenyl-methylene]-6-ethoxycarbonyl-2-indolinone,(f) 3-Z-[1-(4-(N-(2-dimethylamino-ethyl)-N-acetyl-amino)-anilino)-1-phenyl-methylene]-6-ethoxycarbonyl-2-indol(g) 3-Z-[1-(4-(N-(3-dimethylamino-propyl)-N-acetyl-amino)-anilino)-1-phenyl-methylene]-6-ethoxycarbonyl-2-indolinone,(h) 3-Z-[1-(4-(N-(2-dimethylamino-ethyl)-N-methylsulphonyl-amino)-anilino)-1-phenyl-methylene]-6-ethoxycarbonyl-2-indolinone,(i) 3-Z-[1-(4-(dimethylaminomethyl)-anilino)-1-phenyl-methylene]-6-methoxycarbonyl-2-indolinone,(j) 3-Z-[1-(4-(N-acetyl-N-dimethylaminocarbonylmethyl-amino)-anilino)-1-phenyl-methylene]-6-methoxycarbonyl-indolinone,(k) 3-Z-[1-(4-ethylaminomethyl-anilino)-1-phenyl-methylene]-6-methoxycarbonyl-2-indolinone,(l) 3-Z-[1-(4-(1-methyl-imidazol-2-yl)-anilino)-1-phenyl-methylene]-6-methoxycarbonyl-2-indolinone,(m) 3-Z-[1-(4-(N-dimethylaminomethylcarbonyl-N-methyl-amino)-anilino)-1-phenyl-methylene]-6-methoxycarbonyl-indolinone,(n) 3-Z-[1-(4-(N-(2-dimethylamino-ethyl)-N-methylsulphonyl-amino)-anilino)-1-phenyl-methylene]-6-methoxycarbonyl-2-indolinone,(o) 3-Z-[1-(4-(N-(3-dimethylamino-propyl)-N-methylsulphonyl-amino)-anilino)-1-phenyl-methylene]-6-methoxycarbonyl-2-indolinone,(p) 3-Z-[1-(4-(N-dimethylaminocarbonylmethyl-N- ...

METHODS FOR SIMULTANEOUS LEACHING AND EXTRACTION OF PRECIOUS METALS

The present applications relates to methods for the simultaneous leaching and extraction of precious metals. For example, the present application relates to methods of leaching and extracting gold and/or palladium from a substance comprising gold and/or palladium such as a gold- and/or palladium-containing ore in one step using a compound of Formula I:(I). 3. The method of claim 2 , wherein only one of R claim 2 , R claim 2 , Rand Ris H.4. The method of claim 2 , wherein Rand Rtogether with the nitrogen atom to which they are attached form a heterocycloalkyl or a substituted heterocycloalkyl claim 2 , wherein the heterocycloalkyl is selected from aziridinyl claim 2 , azetidinyl claim 2 , pyrrolidinyl claim 2 , piperidinyl claim 2 , azepanyl claim 2 , azocanyl claim 2 , imidazolidinyl claim 2 , oxazolidinyl claim 2 , thiazolidinyl claim 2 , piperazinyl claim 2 , hexahydropyrimidinyl claim 2 , morpholinyl claim 2 , 1 claim 2 ,3-oxazinanyl claim 2 , thiomorpholinyl claim 2 , 1 claim 2 ,3-thiazinanyl claim 2 , 1 claim 2 ,3-diazepanyl claim 2 , 1 claim 2 ,3-oxazepanyl claim 2 , 1 claim 2 ,3-thiazepanyl claim 2 , 1 claim 2 ,4-diazepanyl claim 2 , 1 claim 2 ,4-oxazepanyl claim 2 , 1 claim 2 ,4-thiazepanyl claim 2 , 1 claim 2 ,3-diazocanyl claim 2 , 1 claim 2 ,3-oxazocanyl claim 2 , 1 claim 2 ,3-thiazocanyl claim 2 , 1 claim 2 ,4-diazocanyl claim 2 , 1 claim 2 ,4-oxazocanyl claim 2 , 1 claim 2 ,4-thiazocanyl claim 2 , 1 claim 2 ,5-diazocanyl claim 2 , 1 claim 2 ,5-oxazocanyl and 1 claim 2 ,5-thiazocanyl.5. (canceled)6. The method claim 2 , wherein Ris H and Ris Calkyl or Ccycloalkyl.7. The method of claim 1 , wherein Y is NR.8. The method of claim 7 , wherein Ris H claim 7 , Calkyl or Ccycloalkyl.10. (canceled)11. (canceled)12. The method of claim 1 , wherein the molar ratio of the compound of Formula I to the gold and/or palladium is about 3:1 to about 4:1.13. The method of claim 1 , wherein the acid is HCl having a concentration in the aqueous solution of about 1 M to ...

COMPOUNDS AND METHODS OF TREATING CANCER

Presented herein inter alia are novel compounds and methods of using the same for the treatment of cancers. 2. The compound of having formula (I) claim 1 , wherein Lis a bond.3. The compound of claim 1 , wherein Land Lare bonds.411.-. (canceled)12. The compound of claim 1 , wherein Ris —NRRor substituted or unsubstituted heterocycloalkyl and Ris —NRRor substituted or unsubstituted heterocycloalkyl.13. (canceled)14. The compound of claim 12 , wherein Rand Rare joined to form a substituted or unsubstituted pyrrolidinyl claim 12 , substituted or unsubstituted imidazolidinyl claim 12 , substituted or unsubstituted oxazolidinyl claim 12 , substituted or unsubstituted thiazolidinyl claim 12 , substituted or unsubstituted dioxolanyl claim 12 , substituted or unsubstituted dithiolanyl claim 12 , substituted or unsubstituted piperidinyl claim 12 , substituted or unsubstituted morpholinyl claim 12 , substituted or unsubstituted dioxanyl claim 12 , or substituted or unsubstituted dithianyl claim 12 , substituted or unsubstituted aziridinyl claim 12 , substituted or unsubstituted azetidinyl claim 12 , substituted or unsubstituted azepinyl claim 12 , substituted or unsubstituted oxiranyl claim 12 , substituted or unsubstituted oxetanyl claim 12 , substituted or unsubstituted tetrahydrofuranyl claim 12 , substituted or unsubstituted tetrahydrothiophenyl claim 12 , or substituted or unsubstituted tetrahydropyranyl.15. The compound of claim 14 , wherein Ris —NRR claim 14 , and wherein Rand Rare joined to form a substituted or unsubstituted 5 to 8 membered heterocycloalkyl.16. The compound of claim 15 , wherein Rand Rare joined to form a substituted or unsubstituted pyrrolidine claim 15 , substituted or unsubstituted imidazolidine claim 15 , substituted or unsubstituted oxazolidine claim 15 , substituted or unsubstituted thiazolidine claim 15 , substituted or unsubstituted dioxolane claim 15 , or substituted or unsubstituted dithiolane claim 15 , substituted or unsubstituted ...

NOVEL COMPOUNDS FOR SELECTIVE HISTONE DEACETYLASE INHIBITORS, AND PHARMACEUTICAL COMPOSITION COMPRISING THE SAME

The present invention relates to novel urea derivatives and, more particularly, to novel urea derivatives with histone deacetylase (HDAC) inhibitory activity, isomers thereof, pharmaceutically acceptable salts thereof, their use for the preparation of a medicaments comprising the same, a pharmaceutical composition comprising the same, a treatment method using the composition, and a method for preparing novel urea derivatives. The novel urea derivatives as selective histone deacetylase (HDAC) inhibitors are effective for the treatment of histone deacetylase-mediated diseases such as malignant tumors, inflammatory diseases, rheumatoid arthritis, neurodegeneration, etc. 5. The compound of selected from the group consisting of the following compounds:N-(4-(hydroxycarbamoyl)benzyl)-N-(3-(1-methyl-1H-indazol-5-yl)phenyl)-morpholine-4-carboxamide,N-(4-(hydroxycarbamoyl)benzyl)-4-methyl-N-(3-(1-methyl-1H-indazol-5-yl)-phenyl)piperazine-1-carboxamide,N-(4-(hydroxycarbamoyl)benzyl)-N-(3-(1-methyl-1H-indazol-6-yl)phenyl)-morpholine-4-carboxamide,N-(3-bromophenyl)-N-(4-(hydroxycarbamoyl)benzyl)morpholine-4-carboxamide,N-(3-bromophenyl)-N-(4-(hydroxycarbamoyl)benzyl)-4-methylpiperazine-1-carboxamide,N-(4-(hydroxycarbamoyl)benzyl)-N-(3-(1-methyl-1H-indazol-5-yl)phenyl)-piperidine-1-carboxamide,N-(3-(1H-indol-6-yl)phenyl)-N-(4-(hydroxycarbamoyl)benzyl)morpholine-4-carboxamide,N-(4-(hydroxycarbamoyl)benzyl)-N-(3-(pyridin-3-yl)phenyl)morpholine-4-carboxamide,N-(3-(1H-indol-5-yl)phenyl)-N-(4-(hydroxycarbamoyl)benzyl)morpholine-4-carboxamide,N-(4-(hydroxycarbamoyl)benzyl)-N-phenylmorpholine-4-carboxamide,N-(4-(hydroxycarbamoyl)benzyl)-N-(pyridin-2-yl)morpholine-4-carboxamide,N-(4-(hydroxycarbamoyl)benzyl)-N-(pyridin-3-yl)morpholine-4-carboxamide,4-benzyl-N-(4-(hydroxycarbamoyl)benzyl)-N-(pyrimidin-2-yl)piperazine-1-carboxamide,4-hydroxy-N-(4-(hydroxycarbamoyl)benzyl)-4-phenyl-N-(pyrimidin-2-yl)-piperidine-1-carboxamide,N-(4-(hydroxycarbamoyl)benzyl)-N-(pyrimidin-2-yl)morpholine-4- ...

Ethyl Benzyl Quaternary Amines of Amido Amines for Improved Antifungal properties

Ethyl benzyl quaternaries having superior anti-fungal properties versus their benzyl quaternary analogs. The ethylbenzyl amidoamine quaternaries of the present invention are easily produced without significant waste and with minimal capital, while possessing improved antimicrobial properties.

Bis-Acylated Hydroxylamine Derivatives

The invention provides certain bis-acylated hydroxylamine derivative compounds, pharmaceutical compositions and kits comprising such compounds, and methods of using such compounds or pharmaceutical compositions. In particular, the invention provides methods of using such compounds or pharmaceutical compositions for treating, preventing, or delaying the onset and/or develop of a disease or condition. In some embodiments, the disease or condition is selected from cardiovascular diseases, ischemia, reperfusion injury, cancerous disease, pulmonary hypertension and conditions responsive to nitroxyl therapy. 2. The compound of claim 1 , wherein L is —SO—.3. The compound of claim 1 , wherein Y is aryl substituted with one or more substituents independently selected from W.4. The compound of claim 1 , wherein Y is aryl substituted with one claim 1 , two or three substituents independently selected from W.5. The compound of claim 1 , wherein Y is phenyl substituted with one or more substituents independently selected from W.6. The compound of claim 1 , wherein Y is heteroaryl and said heteroaryl is unsubstituted or substituted with one or more substituents independently selected from W.7. The compound of claim 1 , wherein Y is benzyl and said benzyl is substituted with one or more substituents independently selected from W.8. The compound of claim 1 , wherein W is halo claim 1 , —SORor —NO.9. The compound of claim 1 , wherein W is chloro claim 1 , bromo claim 1 , fluoro or —NO.10. The compound of claim 1 , wherein Rand Rare independently alkyl claim 1 , heterocycloalkyl claim 1 , alkoxy claim 1 , phenyl or benzyloxy claim 1 , wherein said alkyl claim 1 , heterocycloalkyl claim 1 , alkoxy claim 1 , phenyl and benzyoxy are unsubstituted or substituted with one or more substituents independently selected from halo claim 1 , alkyl claim 1 , nitro claim 1 , alkylsulfonyl and trihalomethyl.11. The compound of claim 1 , wherein:{'sup': '1', 'Ris alkyl, heterocycloalkyl, alkoxy, ...

FATTY ACID ANALOGUES AND METHODS OF USE

Provided herein are compounds, pharmaceutical compositions, and methods of treatment for various diseases or conditions, such as cancer. In one aspect, the method comprises the treatment of metastatic cancers. Compounds and methods provided herein are also used for the treatment of diseases such as inflammatory disease, cardiovascular disease, autoimmune disease, and dry eye syndrome. Further provided herein are dietary supplement formulations and methods for supporting a healthy lifestyle. 6. The compound of or , wherein Z is a bond , —NRC(═O)NR— , —NRC(═O)— , —NRC(═O)NR-alkylene- , —NRC(═O)-alkylene-NR— , —NRC(═O)-alkylene- , —NRS(═O)-alkylene- , —NRS(═O)-alkylene-NR— , —(C-Cheteroaryl)- , —NRC(═O)-alkylene-O— , or —OC(═O)NR—.7. The compound of or , wherein Z is a bond.8. The compound of or , wherein Z is —NRC(═O)NR—.9. The compound of or , wherein Z is NRC(═O)NR-alkylene-.10. The compound of , , or , wherein Z is NRC(═O)NR—CH—.11. The compound of or , wherein Z is —NRC(═O)-alkylene-NR—.12. The compound of , , or , wherein Z is —NRC(═O)—CHNR—.13. The compound of or , wherein Z is —(C-Cheteroaryl)-.14. The compound of , , or , wherein Z is triazolyl , tetrazolyl , furanyl , pyrrolyl , thiazolyl , oxazolyl , isoxazolyl , imidazolyl , pyrazolyl , thiadiazolyl , or oxadiazolyl.15. The compound of , , , or , wherein Z is triazolyl.16. The compound of or , wherein Z is —NRC(═O)-alkylene-O—.17. The compound of , , or , wherein Z is —NRC(═O)—CH—O—.18. The compound of or , wherein Z is —OC(═O)NR—.19. The compound of or , wherein Z is —NRS(═O)-alkylene-NR—.20. The compound of , , or , wherein Z is —NRS(═O)—CHCHNR—.21. The compound of any one of - , wherein D is —COH.22. The compound of any one of - , wherein D is —C(═O)NRR.23. The compound of any one of - , wherein D is tetrazolyl.24. The compound of any one of - , wherein R and Rare independently hydrogen , C-Calkyl , C-Ccycloalkyl , or C-Chaloalkyl.25. The compound of any one of - , wherein R and Rare independently ...

SYNTHESIS AND USE OF AMINO LIPIDS

The present invention provides novel amino lipids and a method for synthesizing these compounds. According to the invention, the amino lipids have a structure of the following formula: 118-. (canceled)20. The amino lipid of claim 19 , wherein at least one of Rand Rcan be substituted with a C-Chydrocarbyl group.21. The amino lipid of claim 19 , wherein claim 19 , in connection with Rand R claim 19 , one or more of the C-Calkyl claim 19 , the C-Calkenyl claim 19 , and the C-Calkynyl can be substituted with a C-Chydrocarbyl group.23. The amino lipid of claim 22 , wherein at least one of Rand Rcan be substituted with a C-Chydrocarbyl group.24. The amino lipid of claim 22 , wherein claim 22 , in connection with Rand R claim 22 , one or more of the C-Calkyl claim 22 , the C-Calkenyl claim 22 , and the C-Calkynyl can be substituted with a C-Chydrocarbyl group.27. The amino lipid of claim 26 , wherein at least one of Rand Rcan be substituted with a C-Chydrocarbyl group.29. The amino lipid of claim 28 , wherein claim 28 , in connection with Rand R claim 28 , the C-Calkyl is substituted with a C-Chydrocarbyl group.31. The lipid particle of claim 30 , wherein the lipid particle is a liposome.32. The lipid particle of claim 30 , further containing at least one of a non-cationic lipid claim 30 , a sterol and a bioactive agent claim 30 , wherein the bioactive agent is selected from the group consisting of a nucleic acid claim 30 , an antineoplastic agent claim 30 , an antibiotic claim 30 , an immunomodulator claim 30 , an anti-inflammatory agent claim 30 , an agent acting on a central nervous system claim 30 , a polypeptide and a polypeptoid.33. The lipid particle of claim 30 , wherein the lipid particle is used for delivering a bioactive agent into a cell.34. The lipid particle of claim 30 , wherein the lipid particle is used as a medicament in treatment of at least one of a viral infection claim 30 , a liver disease claim 30 , a liver disorder claim 30 , and a cancer.36. The ...

HYDROGEN SULFIDE DONOR IN ORGANIC SALT FORM AND PREPARATION METHOD THEREFOR

A hydrogen sulfide donor in an organic salt form and a preparation method thereof. The hydrogen sulfide donor exists as a salt formed by organic compounds with an alkaline motif and hydrogen sulfide with weak acidity. The hydrogen sulfide donor features with a simple structure, and an easy preparation method. Moreover, hydrogen sulfide donors in different forms can be prepared according to research and development needs. After the hydrogen sulfide donor enters an organism, the process of in vivo dissociation and hydrogen sulfide supply is simple, rapid, and effective, and there is no requirement for enzyme or any other complicated condition, and thus, the hydrogen sulfide donor has a great application prospect and value. 1. A hydrogen sulfide donor in organic salt form , characterized in that the donor is a salt structure formed by organic compounds with basic moiety and hydrogen sulfide.2. The hydrogen sulfide donor in organic salt form according to claim 1 , characterized in that said organic compounds having basic moiety are those pharmacological compounds possessing physiological and/or pharmacological activities.3. The hydrogen sulfide donor in organic salt form according to claim 1 , characterized in that said organic compounds having basic moiety are those with the structures selected from the group consisting of guanidines claim 1 , amidines claim 1 , hydrazines.4. The hydrogen sulfide donor in organic salt form according to claim 1 , characterized in that said organic compounds having basic moiety are those amino acid compounds such as arginine claim 1 , lysine claim 1 , etc.5. The hydrogen sulfide donor in organic salt form according to claim 1 , characterized in that said organic compounds having basic moiety are alkaloids.6. A preparative method for hydrogen sulfide donor in organic salt form according to claim 1 , characterized in that said organic compounds having basic moiety are dissolved in the solvent claim 1 , to which is added hydrogen sulfide ...

Novel Triarylethylene Compounds and Methods Using Same

The present invention includes compounds useful in preventing or treating cancer in a subject in need thereof. The present invention also includes methods of preventing or treating cancer in a subject in need thereof by administering to the subject a therapeutically effective amount of a compound of the invention. 2. The compound of claim 1 , wherein Ris selected from the group consisting of H claim 1 , methyl claim 1 , —(CH)OH claim 1 , —(CH)OS(O)CH claim 1 , —(CH)N claim 1 , —(CH)NH claim 1 , and —(CH)N(CH).3. The compound of claim 1 , wherein X is N(R)(R).4. The compound of claim 3 , wherein either Rand Rare each H or Ris H and Ris —C(O)R.5. The compound of claim 1 , wherein m is 0 claim 1 , n is 0 claim 1 , and p is 0.7. A composition comprising a compound of .8. The composition of claim 7 , wherein the composition further comprises a pharmaceutically acceptable carrier.9. The composition of claim 7 , wherein the composition further comprises an additional therapeutic agent.11. The method of claim 10 , wherein Ris selected from the group consisting of H claim 10 , methyl claim 10 , —(CH)OH claim 10 , —(CH)OS(O)CH claim 10 , —(CH)N claim 10 , —(CH)NH claim 10 , and —(CH)N(CH).12. The method of claim 10 , wherein X is N(R)(R).13. The method of claim 12 , wherein either Rand Rare each H or Ris H and Ris —C(O)R.14. The method of claim 10 , wherein m is 0 claim 10 , n is 0 claim 10 , and p is 0.16. The method of claim 10 , wherein the cancer is selected from the group consisting of lung cancer claim 10 , colon cancer claim 10 , melanoma claim 10 , breast cancer claim 10 , ovarian cancer claim 10 , prostate cancer claim 10 , liver cancer claim 10 , pancreatic cancer claim 10 , a CNS tumor claim 10 , neuroblastoma claim 10 , leukemia claim 10 , bone cancer claim 10 , intestinal cancer claim 10 , lymphoma claim 10 , and combinations thereof.17. The method of claim 10 , wherein the method further comprises administering to the subject at least one additional therapeutic ...

INK, INK CARTRIDGE, INK JET RECORDING DEVICE, INK JET INK PRINTED MATTER, COMPOUND, AND COMPOSITION

Ink contains at least one of a compound represented by the following chemical formula 1, a compound represented by chemical formula 2, a compound represented by chemical formula 3, or a compound represented by chemical formula 4. 2. The ink according to claim 1 , wherein Rrepresents a cycloalkyl group claim 1 , an aryl group claim 1 , or an aralkyl group.5. The ink according to claim 4 , wherein Ris a group represented by —COOX claim 4 , where Xrepresents a hydrocarbon group having 1 to 10 carbon atoms6. An ink cartridge comprising:{'claim-ref': {'@idref': 'CLM-00001', 'claim 1'}, 'the ink of ; and'}{'claim-ref': {'@idref': 'CLM-00001', 'claim 1'}, 'a container to accommodate the ink of .'}7. An ink jet recording device comprising:{'claim-ref': {'@idref': 'CLM-00001', 'claim 1'}, 'a discharging device to discharge the ink of .'}8. An ink jet ink printed matter comprising:{'claim-ref': {'@idref': 'CLM-00001', 'claim 1'}, 'an image of the ink of ; and'}a recording medium on which the image is formed.10. A composition comprising:{'claim-ref': {'@idref': 'CLM-00009', 'claim 9'}, 'the compound of .'} This patent application is based on and claims priority pursuant to 35 U.S.C. §119 to Japanese Patent Application Nos. 2013-118869 and 2014-057602, on Jun. 5, 2013 and Mar. 20, 2014, respectively, in the Japan Patent Office, the entire disclosures of which are hereby incorporated by reference herein.1. Technical FieldThe present invention relates to ink, an ink cartridge, an ink jet recording device, an ink jet ink printed matter, a compound, and a composition.2. Background ArtAn ink jet recording system is known as a method of forming an image on a recording medium, typically paper. The ink jet recording system has an excellent consumption efficiency and excellent resource saving properties, resulting in low cost of ink per recording unit.In recent years, ink jet recording system using ultraviolet curing ink has become appealing.JP-2009-67926-A discloses an ink composition ...

RECEPTOR INHIBITORS, PHARMACEUTICAL COMPOSITIONS COMPRISING THE SAME AND USE THEREOF

The present invention discloses a receptor inhibitor of formula (I), a composition comprising the same and the usage thereof. 2. The compound according to claim 1 , or a pharmaceutically acceptable salt claim 1 , ester claim 1 , stereoisomer claim 1 , polymorph claim 1 , solvate claim 1 , N-oxide claim 1 , isotopically labeled compound claim 1 , metabolite claim 1 , or prodrug thereof claim 1 , wherein R claim 1 , R claim 1 , X claim 1 , R claim 1 , Rand Xhave the definitions described in the Meaning (4).3. The compound according to claim 2 , or a pharmaceutically acceptable salt claim 2 , ester claim 2 , stereoisomer claim 2 , polymorph claim 2 , solvate claim 2 , N-oxide claim 2 , isotopically labeled compound claim 2 , metabolite or prodrug thereof claim 2 , wherein R claim 2 , Rand Rare each independently selected from the group consisting of H claim 2 , halogen claim 2 , cyano claim 2 , nitro claim 2 , Calkyl claim 2 , Calkenyl claim 2 , Calkynyl claim 2 , Ccyclic hydrocarbyl group claim 2 , 3- to 10-membered heterocyclic group claim 2 , Caryl claim 2 , 5- to 14-membered heteroaryl claim 2 , Caralkyl claim 2 , —OR claim 2 , —SR claim 2 , —OC(═O)R claim 2 , —C(═O)R claim 2 , —C(═O)OR claim 2 , —C(═O)NR—OH claim 2 , —C(═O)NRR claim 2 , —C(═O)NRS(═O)NRR claim 2 , —C(═O)NRS(═O)R claim 2 , —S(═O)R claim 2 , —S(═O)OR claim 2 , —S(═O)NRR claim 2 , —S(═O)NRS(═O)OR claim 2 , —S(═O)NRC(═O)R claim 2 , —S(═O)NRC(═O)OR claim 2 , —NRR claim 2 , —NR—C(═O)R claim 2 , —NR—C(═O)OR claim 2 , —NR—S(═O)—R claim 2 , —NR—C(═O)—NRR claim 2 , —Calkylene-OR claim 2 , —Calkylene-OC(═O)R claim 2 , —Calkylene-C(═O)OR claim 2 , —Calkylene-S(═O)R claim 2 , —Calkylene-S(═O)OR claim 2 , —Calkylene-OC(═O)NRR claim 2 , —Calkylene-C(═O)NRR claim 2 , —Calkylene-C(═O)NR—S(═O)R claim 2 , —Calkylene-NR—C(═O)NRR claim 2 , —Calkylene-OS(═O)R claim 2 , —Calkylene-OS(═O)NRR claim 2 , —Calkylene-S(═O)NRR claim 2 , —Calkylene-NR—S(═O)NRR claim 2 , —Calkylene-NRRand —O—Calkylene-NRR.6. (canceled)8. ( ...

HETEROCYCLICALKYL DERIVATIVE COMPOUNDS AS SELECTIVE HISTONE DEACETYLASE INHIBITORS AND PHARMACEUTICAL COMPOSITIONS COMPRISING THE SAME

The present invention relates to novel heterocyclicalkyl derivatives having histone deacetylase (HDAC) inhibitory activity, optical isomers thereof or pharmaceutically acceptable salts thereof, the use thereof for the preparation of medicaments, pharmaceutical compositions containing the same, a method for treating diseases using the composition, and methods for preparing the novel heterocyclicalkyl derivatives. The novel heterocyclicalkyl derivatives according to the present invention are selective histone deacetylase (HDAC) inhibitors, and may be effectively used for the treatment of histone deacetylase-mediated diseases, such as cell proliferative diseases, inflammatory diseases, autosomal dominant diseases, genetic metabolic diseases, autoimmune diseases, acute/chronic neurological disease, hypertrophy, heart failure, ocular diseases, or neurodegenerative diseases. 6. A pharmaceutical composition for preventing or treating histone deacetylase-mediated disease claim 1 , comprising claim 1 , as an active ingredient claim 1 , the compound represented by formula I claim 1 , optical isomer thereof or pharmaceutically acceptable salt thereof according to .7. The pharmaceutical composition of claim 6 , wherein the histone deacetylase-mediated disease is cell proliferative disease claim 6 , inflammatory disease claim 6 , autosomal dominant disease claim 6 , genetic metabolic disease claim 6 , autoimmune disease claim 6 , acute/chronic neurological disease claim 6 , hypertrophy claim 6 , heart failure claim 6 , ocular disease claim 6 , or neurodegenerative disease.8. A method for treating histone deacetylase-mediated disease claim 1 , comprising administering a therapeutically effective amount of the compound represented by formula I claim 1 , optical isomer thereof or pharmaceutically acceptable salt thereof according to .9. (canceled) The present invention relates to novel heterocyclicalkyl derivatives, and more particularly to novel heterocyclicalkyl derivatives ...

ANTIMICROBIAL COMPOUNDS, COMPOSITIONS AND METHODS

The invention discloses compounds of the formula wherein A, B, X, Y and Z are defined. The compounds of the invention show activity against a range of bacteria, and are useful in the treatment or prophylaxis of a bacterial infection in an animal. 2. The compound of claim 1 , wherein A is an aryl group selected from a group consisting of phenyl claim 1 , thiazolyl claim 1 , pyridyl claim 1 , imidazolyl claim 1 , and benzothiazole.3. The compound of wherein A is a phenyl group claim 1 , optionally substituted with from one to three groups independently selected from a group consisting of halo claim 1 , C1-C6 alkyl claim 1 , C1-C6 haloalkyl claim 1 , C1-C6 alkoxy claim 1 , C1-C6 haloalkoxy claim 1 , nitro claim 1 , cyano and C1-C6 thioalkyl.5. The compound of claim 1 , wherein B is an aryl group selected from a group consisting of phenyl claim 1 , thiazolyl claim 1 , pyridyl claim 1 , and benzothiazole.6. The compound of claim 5 , wherein B is a phenyl group claim 5 , optionally substituted with from one to three groups independently selected from a group consisting of halo claim 5 , C1-C6 alkyl claim 5 , C1-C6 haloalkyl claim 5 , C1-C6 alkoxy claim 5 , C1-C6 haloalkoxy claim 5 , nitro claim 5 , cyano and C1-C6 thioalkyl.7. The compound of claim 1 , wherein Y is CH═N.8. The compound of claim 1 , wherein Ris NR claim 1 , with Ras defined in .9. The compound of claim 8 , wherein Ris H.10. The compound of claim 1 , wherein R claim 1 , Rand Rare all H.11. The compound of which is one of 1-[({3-[(2 claim 1 ,3-dichlorophenyl)methoxy]phenyl}methylidene)amino]guanidine; 1-{[(3-{[2-chloro-3-(trifluoromethyl)phenyl]methoxy}phenyl)methylidene]amino} guanidine; 7-[(2 claim 1 ,3-dichlorophenyl)methoxy]-1 claim 1 ,2 claim 1 ,3 claim 1 ,4-tetrahydroisoquinoline-2-carboximidamide; 5-[(2 claim 1 ,3-dichlorophenyl)methoxy]-1 claim 1 ,2 claim 1 ,3 claim 1 ,4-tetrahydroisoquinoline-2-carboximidamide; 1-({3-[(2 claim 1 ,3-dichlorophenyl)methoxy]phenyl}methyl)-1-methylguanidine; 1-({3-[(2 ...

SUBSTITUTED CARBOXYLIC ACID DERIVATIVES AS AGGRECANASE INHIBITORS FOR THE TREATMENT OF OSTEOARTHRITIS

The present invention relates to compounds of the formula I and in particular medicaments comprising at least one compound of the formula I for use in the treatment and/or prophylaxis of physiological and/or pathophysiological states in the triggering of which ADAMTS5 is involved, in particular for use in the treatment and/or prophylaxis of osteoarthritis, hepatocirrhosis, traumatic cartilage injuries, pain, allodynia or hyperalgesia. 5. Compounds selected from the group consisting ofa) 4-[(Biphenyl-4-carbonyl)-amino]-2-methyl-4-(3,4,5-trimethoxy-benzylcarbamoyl)-butyric acidb) (2S,4S)-4-[2-(4-Fluoro-phenyl)-1,1-dimethyl-ethylcarbamoyl]-4-{[5-(4-fluoro-phenyl)-thiazole-2-carbonyl]-amino}-2-methyl-butyric acidc) (2S,4S)-4-[(Biphenyl-4-carbonyl)-amino]-4-[(S)-2-(4-fluoro-phenyl)-1-methyl-ethylcarbamoyl]-2-methyl-butyric acidd) (2S,4S)-4-[(Biphenyl-4-carbonyl)-amino]-4-(1,1-dimethyl-2-pyridin-3-yl-ethylcarbamoyl)-2-methyl-butyric acide) (2S,4S)-4-[(Biphenyl-4-carbonyl)-amino]-4-[2-(4-fluoro-phenyl)-1,1-dimethyl-ethylcarbamoyl]-2-methyl-butyric acidf) (2S,4S)-2-Benzyl-4-[(biphenyl-4-carbonyl)-amino]-4-[2-(4-fluoro-phenyl)-1,1-dimethyl-ethylcarbamoyl]-butyric acidg) (2S,4S)-2-[(Biphenyl-4-carbonyl)-amino]-2-[2-(4-fluoro-phenyl)-1,1-dimethyl-ethylcarbamoyl]-ethyl}-pentanoic acidh) (2S,4S)-4-[(Biphenyl-4-carbonyl)-amino]-4-[2-(4-fluoro-phenyl)-1,1-dimethyl-ethylcarbamoyl]-2-methoxymethyl-butyric acidi) (2S,4S)-4-[2-(4-Fluoro-phenyl)-1,1-dimethyl-ethylcarbamoyl]-2-methyl-4-[4-(1-methyl-1H-pyrazol-3-yl)-benzoylamino]-butyric acidj) (2S,4S)-4-[2-(4-Fluoro-phenyl)-1,1-dimethyl-ethylcarbamoyl]-2-methyl-4-(4-pyridin-2-yl-benzoylamino)-butyric acidk) (2S,4S)-4-[(3-Fluoro-biphenyl-4-carbonyl)-amino]-4-[2-(4-fluoro-phenyl)-1,1-dimethyl-ethylcarbamoyl]-2-methyl-butyric acidl) (2S,4S)-4-[2-(4-Fluoro-phenyl)-1,1-dimethyl-ethylcarbamoyl]-4-{[1-(4-fluoro-phenyl)-piperidine-4-carbonyl]-amino}-2-methyl-butyric acidm) 4-[2-(4-Fluoro-phenyl)-1,1-dimethyl-ethylcarbamoyl]-2-methyl-4-[(5- ...

Piperazine derivatives and process for the preparation thereof

The present invention relates to novel compound having strong antitumor activities of general formula (I), wherein R1 and R2 are independently hydrogen, substituted or unsubstituted C1-C8 alkyl, substituted or unsubstituted C3-C6 cycloalkyl, substituted or unsubstituted C2-C8 unsaturated alkyl, ketone, substituted or unsubstituted aryl, substituted or unsubstituted C1-C4 alkoxy, substituted or unsubstituted arylhydroxy, substituted or unsubstituted amino, C1-C4 lower ester, C1-C4 lower thioester, thiol, substituted or unsubstituted carboxyl, epoxy, substituted or unsubstituted C1-C4 lower thioalkoxy; or R1 and R2 are fused to form C3-C4 saturated or unsaturated chain; R3, R4, R5, R6 and R7 are independently hydrogen, halogen, hydroxy, nitro, C1-C4 lower ester, C1-C4 lower alkyl, C1-C4 lower thioalkyl, substituted or unsubstituted C3-C6 cycloalkyl, C1-C4 lower alkoxy, C1-C4 lower thioalkoxy, substituted or unsubstituted aryl, substituted or unsubstituted lower arylalkoxy, substituted or unsubstituted lower alkylamino, or lower alkyl substituted or unsubstituted carbamate; or among R3, R4, R5, R6 and R7, two adjacent groups are bonded with each other to form 1,2-phenylene or 2,3-naphthylene; X is oxygen, sulfur, or substituted or unsubstituted imino; Y is bonded at the 3-position or 4-position of the aromatic ring part wherein Y is oxygen or -NR8- (wherein, R8 is the same with the above-mentioned R3); Z is hydroxy, C1-C4 lower alkoxy, C1-C4 lower thioalkoxy, substituted or unsubstituted aryloxy, C1-C4 lower alkylamino, substituted or unsubstituted cycloamino containing 1-5 nitrogen atoms; A is nitrogen or -CH=; its pharmaceutically acceptable acid addition salts and process for the preparation thereof.

Methods for selective leaching and extraction of precious metals in organic solvents

The present application relates to methods for leaching and extraction of precious metals. For example, the present application relates to methods of leaching gold, palladium and/or platinum from a substance comprising gold, palladium and/or platinum (such as a gold-containing ore or a platinum group metal (PGM) concentrate) using an organic solvent that is water-miscible or partially water-miscible.

Cathepsin S inhibitors

Cathepsin S inhibitors having formula (I), (II), (III) or (IV) as shown in the specification. These inhibitors can be used to treat cancer and autoimmune/inflammatory diseases.

Biguanide compound and use thereof

Salze der Pyromellitsäure, ein Verfahren zu ihrer Herstellung sowie deren Verwendung

Preparation of substituted cyanoguanidine

Bis(1-substituted biguanide) derivatives

A bis(1-substituted biguanide) derivative of the formula: R.sup.3 R.sup.4 N.C(:NR.sup.5)NH.C(NR.sup.9)NR.sup.1 --X--NR 2 .C(:NR 9 )NH.C(:NR 6 )--NR 7 R 8 V or a tautomeric form thereof, wherein R 1 , R 2 and R 9 , which may be the same or different, are each hydrogen, a 1-16C alkyl radical, a 3-16C cycloalkyl radical, a (3-12C cycloalkyl)-(1-4C alkyl) radical, an optionally substituted phenyl or naphthyl radical, an optionally substituted phenyl(1-4C)alkyl or naphthyl(1-4C)alkyl radical or an optionally substituted diphenylmethyl radical, provided that at least one of R 1 , R 2 and R 9 is other than hydrogen; R 3 , R 4 , R 7 and R 8 , which may be the same or different are each hydrogen, or an alkyl, cycloalkyl, (cycloalkyl)alkyl, phenyl, naphthyl, phenylalkyl, naphthylalkyl, or diphenylmethyl radical as defined above, or a 2-16 alkoxyalkyl radical, or R 3 , R 4 and the nitrogen atom to which they are attached, or R 7 and R 8 and the nitrogen atom to which they are attached, which may be the same or different, are each a 1-azetidinyl, 1-pyrrolidinyl, piperidino, hexamethyleneimino, heptamethyleneimino, morpholino or 4-(1-8C alkanoyl)-1-piperazinyl radical, each of which may bear 1-3C alkyl substituents; R 5 and R 6 , which may be the same or different, are each hydrogen or a 1-8C alkyl radical; and X is a 2-16C linking group which is a straight chain alkylene radical, or a straight chain alkylene radical bearing one or more 1-16C alkyl substituents, of which any pair or pairs which are attached to different carbon atoms, may be joined so as to form, together with the intervening carbon atom or atoms of the alkylene radical, a (5-7C)-cycloalkyl radical or radicals; and the acid addition salts thereof, processes for their manufacture, and antibacterial and antifungal compositions and methods using said compounds.

Salts of pyromellitic acid, a process for their preparation, and their use

The invention relates to salts of pyromellitic acid which comprise 1 mol of pyromellitic acid and 0.5. to 2 mol of a guanidine of the following composition: ##STR1## in which R, R 1 , R 2 , R 3 and R 4 are identical or different radicals from the group consisting of hydrogen, alkyl, cycloalkyl and aromatic hydrocarbon residues having 1 to 8 carbon atoms, and R 1 and R 2 and R 3 and R 4 may form a joint ring which may contain an oxygen atom as heteroatom. Also claimed are the preparation of the salts and their use for matt epoxide and hybrid powder coatings.

氨基甲酰肟化合物以及含有该化合物的聚合引发剂及聚合性组合物

本发明的课题在于提供在溶剂中的溶解性高并且具有令人满意的感度(碱产生能力)的化合物、含有该化合物作为聚合引发剂而成的聚合性组合物以及其固化物。本发明提供下述式(I)所表示的氨基甲酰肟化合物。进而，本发明提供包含该化合物的聚合引发剂、含有该聚合引发剂及聚合性化合物的聚合性组合物、其固化物以及其制造方法。式中的符号的定义参照说明书。

Derivatives of piperazine and method of their synthesis

FIELD: organic chemistry and technology. SUBSTANCE: invention relates to new compounds of the general formula (I) where values R 1 -R 7 , A, Z, Y and X are given in p. 1 of the invention claim. Compounds show the strong antitumor activity. Invention describes the method of their synthesis also. EFFECT: improved method of synthesis, antitumor properties. 3 cl, 4 tbl, 235 ex (19) 13) ВИ "” 2 146 254 ' (51) МПК? СЛ С 07 0 295/104, 295/112, А 61 К 31/495 РОССИЙСКОЕ АГЕНТСТВО ПО ПАТЕНТАМ И ТОВАРНЫМ ЗНАКАМ 12) ОПИСАНИЕ ИЗОБРЕТЕНИЯ К ПАТЕНТУ РОССИЙСКОЙ ФЕДЕРАЦИИ (21), (22) Заявка: 98105684/04, 28.06.1997 (71) Заявитель: Самдзин Фармасьютикал Ко., Лтд. (КК) (24) Дата начала действия патента: 28.06.1997 (72) Изобретатель: Еуй-Хван Чо (КК), (30) Приоритет: 29.06.1996 КК 1996/25825 Сун-Ган Чунг (КК), Сун-Хван Ли (КБ), Хо-Сеок 29.06.1996 29.06.1996 18.09.1996 03.06.1997 03.06.1997 04.06.1997 04.06.1997 1996/25826 1996/25827 1996/40596 1997122984 1997122985 1997123192 1997123193 Квон (КК), Дзае-Еунг Ли (КК), Донг-Вук Канг (КК), Дзеонг-Хо Дзоо (КК), Янг-Хи Ли (КК) (73) Патентообладатель: Самдзин Фармасьютикал Ко., Лтд. (КК) С1 па (46) Дата публикации: 10.03.2000 (56) Ссылки: ЕР 0486734 АЛ, 1990. ЗЦ 551871 А, 1981. ЕР 0128007 АЗ, 1984. (85) Дата перевода заявки РСТ на национальную фазу: 30.03.1998 (86) Заявка РСТ: КК 97/00128 (28.06.1997) 2146254 (87) Публикация РСТ: М/О 98/00402 (08.01.1998) (98) Адрес для переписки: 129010, Москва, ул.Б.Спасская, 25, стр.3, ООО "Городисский и Партнеры" Лебедевой Н.Г. КО (54) ПРОИЗВОДНЫЕ ПИПЕРАЗИНА И СПОСОБ ИХ ПОЛУЧЕНИЯ (57) Реферат: Изобретение относится к новым соединениям, обладающим СИЛЬНОЙ противоопухолевой активностью, В отвечающим общей формуле (1), где значения 2. и К. - Вр, А, А, У, Х указаны в п.1 формулы. Описывается также способ их получения. 3 УУЗСЭ9УЬС Го с.п.Ф-лы, 4 табл. ЗСУ ЕСс ПЧ Го (19) 13) ВИ "” 2 146 254 ' (51) 1пЁ. С1.7 СЛ К 31/495 С 07 0 295/104, 295/112, А 61 КУЗЗАМ АСЕМСУ ГОК РАТЕМТ$ АМО ТКАОЕМАКК$ 12) АВЗТКАСТ ОЕ ...

偶氮介体

本申请涉及偶氮化合物和它们作为诊断方法中的介体的用途。本申请还涉及包含这类偶氮化合物的检测试剂、试剂盒和测试元件。

관능성 중합체 및 그의 제조방법

내용 없음.

Novel piperazine derivatives and their preparation method

본 발명은 다음의 일반구조식 (I)로 표시되는 화합물 및 그 제약학적으로 허용되는 산 부가염에 관한 것이다. The present invention relates to a compound represented by the following general formula (I) and a pharmaceutically acceptable acid addition salt thereof. [일반구조식 1] [General Structural Formula 1] R 3 , R 4 , R 5 , R 6 , R 7 및 R 8 은 각각 수소원자, 할로겐원자, 하이드록시기, 니트로기, C 1 -C 4 의 저급에스테르기, C 1 -C 4 의 저급알킬기, C 3 -C 8 의 치환 또는 비치환의 3-6원의 사이클로알킬기, C 1 -C 4 의 저급알콕시기, C 1 -C 4 의 저급티오알콕시기, 치환 또는 비치환의 아릴기, 치환 또는 비치환의 아릴저급알콕시기, 치환 또는 비치환의 저급알킬아미노기, 또는 저급알킬치환 또는 비치환의 카바메이트기이며, X는 산소원자, 유황원자, 치환 또는 비치환의 아민기이며, Z는 수소원자, 하이드록시기, C 1 -C 4 의 저급알콕시기, C 1 -C 4 의 저급티오알콕시기, 치환된 아릴옥시기, C 1 -C 4 의 저급알킬아민기, 질소원자 1 내지 5개까지를 함유할 수 있는 환상아민기, 치환된 피리딘기 그리고 치환된 티오펜기 등을 의미한다. R 3, R 4, R 5 , R 6, R 7 and R 8 are each a hydrogen atom, a halogen atom, a hydroxyl group, a nitro group, a lower ester of a C 1 -C 4, a lower alkyl group of C 1 -C 4 , a substituted C 3 -C 8 cycloalkyl or unsubstituted 3-6 circle alkyl group, a lower thioalkoxy group, a substituted or unsubstituted aryl group, a substituted or unsubstituted lower alkoxy group of C 1 -C 4, C 1 -C 4 An aryl lower alkoxy group of a ring, a substituted or unsubstituted lower alkylamino group, or a lower alkyl substituted or unsubstituted carbamate group, X is an oxygen atom, a sulfur atom, a substituted or unsubstituted amine group, Z is a hydrogen atom, a hydroxy group , C 1 -C 4 lower alkoxy group, C 1 -C 4 lower thioalkoxy group, substituted aryloxy group, C 1 -C 4 lower alkylamine group, may contain up to 1 to 5 nitrogen atoms Cyclic amine group, substituted pyridine group and substituted thiophene group. 본 발명에 따른 화합물은 탁월한 항암활성을 가지며 그 독성이 매우 낮아 항암제로서 우수한 효과가 기대된다. The compound according to the present invention has excellent anticancer activity and its low toxicity is expected to be an excellent anticancer agent.

一种不对称硫脲类化合物的制备方法

本发明公开了一种不对称硫脲类化合物的制备方法，包括：在DMSO或DMF溶剂中，以胺类化合物与二硫化碳为底物，合成不对称硫脲类化合物。本发明方法通过三组份串联反应一步合成不对称硫脲类化合物。本发明反应原料廉价易得，制备方法简单。反应仅需要溶剂，不需要其它添加剂，产率高，操作简单，适用于不同类型的不对称硫脲类化合物的合成。本发明方法可用于合成一系列的不对称硫脲类化合物，合成的产物不仅可作为中间化合物，用于进一步构筑复杂的活性化合物；同时该类化合物具有极大的药物活性潜力。

Copolymers for compositions sensitive in near infrared region of radiation for covering positive thermal lithographic printing forms

FIELD: chemistry. SUBSTANCE: claimed invention relates to thermal lithographic printing forms and their coatings. Described is polymer, which has general formula, presented below, where a, b, c and d are molar ratios, varying between approximately 0.01 and approximately 0.90; A1 represents monomer units, containing cyano-containing suspended group, in which cyano is not bound directly to main copolymer chain; A2 contains suspended group, containing 5,5-dialkylhydantoin group, aminosulphonamide group or hydroxygroup; A3 contains alkyl or aryl suspended group, aryl is eventually substituted alkyl; and A4 contains suspended group, containing group of carboxylic acid. Formula . EFFECT: provision of high rate of laser image formation, high resolution image, wide processing possibilities, stable storage term, good resistance to impact of chemical substances and long run on printing machine. 10 cl, 21 ex, 1 tbl РОССИЙСКАЯ ФЕДЕРАЦИЯ (19) RU (51) МПК C08F 220/10 C08F 220/36 C08F 220/38 C08F 220/54 C08F 212/02 (11) (13) 2 559 050 C2 (2006.01) (2006.01) (2006.01) (2006.01) (2006.01) ФЕДЕРАЛЬНАЯ СЛУЖБА ПО ИНТЕЛЛЕКТУАЛЬНОЙ СОБСТВЕННОСТИ (12) ОПИСАНИЕ (21)(22) Заявка: ИЗОБРЕТЕНИЯ К ПАТЕНТУ 2012153993/04, 14.09.2010 (24) Дата начала отсчета срока действия патента: 14.09.2010 (43) Дата публикации заявки: 20.06.2014 Бюл. № 17 (73) Патентообладатель(и): МАЙЛАН ГРУП (VN) R U Приоритет(ы): (22) Дата подачи заявки: 14.09.2010 (72) Автор(ы): НГУЙЕН Ми Т. (CA), ПХАН Акха (VN), НГУЙЕН-ТРУОНГ Вьет-Тху (VN), ЛОКА Марк-Андре (CA) (45) Опубликовано: 10.08.2015 Бюл. № 22 (85) Дата начала рассмотрения заявки PCT на национальной фазе: 13.12.2012 2 5 5 9 0 5 0 (56) Список документов, цитированных в отчете о поиске: WO 2008048749 A2, 24.04.2008. EP 0001136886 A1, 26.09.2001 . US 20080139737 A1, 12.06.2008. STN RN 346587-51-7 от 18.07.2001. JP 62063595, 20.03.1987. US 20080139737 A1, 12.06.2008. GB 780284, 31.07.1957. EA 2658 B1, 29.08.2002. RU 2158278, 27.10.2000 CA 2010/001401 (14.09.2010) C 2 C 2 ...

Copolymers, polymeric particles comprising said copolymers and copolymeric binders for radiation-sensitive coating compositions for negative-working radiation-sensitive lithographic printing plates

Copolymers for near-infrared radiation-sensitive coating compositions for positive-working thermal lithographic printing plates

Substituted phenoxyurea, its preparation, herbicide containing same as an active intredient

(57)【要約】本公報は電子出願前の出願データであるた め要約のデータは記録されません。

The thermoplastic compounds of CBA and heat-swellable

本发明涉及一种化学发泡剂，其包含至少一种氨基甲酸叔烷基酯。该化学发泡剂可以热活化，并且适于热塑性泡沫材料和可以例如引入用于汽车制造和建筑物绝缘的可热膨胀的挡板和/或增强元件中。

A kind of preparation method of asymmetry thiourea

本发明公开了一种不对称硫脲类化合物的制备方法，包括：在DMSO或DMF溶剂中，以胺类化合物与二硫化碳为底物，合成不对称硫脲类化合物。本发明方法通过三组份串联反应一步合成不对称硫脲类化合物。本发明反应原料廉价易得，制备方法简单。反应仅需要溶剂，不需要其它添加剂，产率高，操作简单，适用于不同类型的不对称硫脲类化合物的合成。本发明方法可用于合成一系列的不对称硫脲类化合物，合成的产物不仅可作为中间化合物，用于进一步构筑复杂的活性化合物；同时该类化合物具有极大的药物活性潜力。

Novel piperazine derivatives and preparation method thereof

본 발명은 다음의 일반구조식(Ⅰ)로 표시되는 화합물 및 그 제약학적으로 허용되는 산부가염에 관한 것이다. R 3 , R 4 , R 5 , R 6 , R 7 및 R 8 은 각각 수소원자, 할로겐원자, 하이드록시기, 니트로기, C 1 -C 4 의 저급에스테르기, C 1 -C 4 의 저급알킬기, C 3 -C 8 의 치환 또는 비치환의 3-6원의 사이클로알킬기, C 1 -C 4 의 저급알콕시기, C 1 -C 4 의 저급티오알콕시기, 치환 또는 비치환의 아릴기, 치환 또는 비치환의 아릴저급알콕시기, 치환 또는 비치환의 저급알킬아미노기, 또는 저급알킬치환 또는 비치환의 카바메이트기이며, X는 산소원자, 유황원자, 치환 또는 비치환의 아민기이며, Z는 수소원자, 하이드록시기, C 1 -C 4 의 저급알콕시기, C 1 -C 4 의 저급티오알콕시기, 치환된 아릴옥시기, C 1 -C 4 의 저급알킬아민기, 질소원자 1 내지 5까지를 함유할 수 있는 환상아민기, 치환된 피리딘기 그리고 치환된 티오펜기 등을 의미한다. 본 발명에 따른 화합물은 탁월한 항암활성을 가지며 그 독성이 매우 낮아 항암제로서의 우수한 효과가 기대된다.

Finely divided blocked isocyanates prepared in the presence of surfactants

A process for the preparation of blocked polyisocyanate powders consisting of reacting the polyisocyanate and blocking agent in solution in the presence of a surfactant, whereby the product precipitates in extremely finely divided form.

Ink, ink cartridge, ink jet recording device, ink jet ink printed matter, compound, and composition

Ink contains at least one of a compound represented by the following chemical formula 1, a compound represented by chemical formula 2, a compound represented by chemical formula 3, or a compound represented by chemical formula 4.

Ink, ink cartridge, ink jet recording device, ink jet ink printed matter, compound, and composition

Ink contains at least one of a compound represented by the following chemical formula 1, a compound represented by chemical formula 2, a compound represented by chemical formula 3, or a compound represented by chemical formula 4.

Ink, ink cartridge, ink jet recording device, ink jet ink printed matter, compound, and composition

Ink contains at least one of a compound represented by the following chemical formula 1, a compound represented by chemical formula 2, a compound represented by chemical formula 3, or a compound represented by chemical formula 4.

Asthma treatment by inhalation of micronized N,N-diethyl-4-methyl-1-piperazinecarboxamide pamoate

Asthma is effectively treated by inhalation of powder dispensed from an aerosol suspension of powdered N,N-diethyl-4-methyl-1piperazinecarboxamide pamoate, which is dispersed as a fine powder, essentially below 10 microns in particle size, which gives an improved ratio of absorption in the lungs as compared to systemic absorption.

N1-cyclic amine-n2-substituted biguanide derivatives, methods of preparing the same and pharmaceutical composition comprising the same

본 발명은 하기 화학식 1로 표시되는 N1-고리아민-N2-치환된 바이구아나이드 유도체 또는 그의 약학적으로 허용가능한 염, 이의 제조방법 및 이를 유효성분으로 하는 약학 조성물을 제공한다. 본 발명의 바이구아나이드 유도체는 기존 약물에 비해 적은 복용량으로도 에너지 대사 조절에 관여하는 AMPK가 우수한 활성화 효과를 나타냄으로써, 암세포 증식 억제 효과 및 암의 재발과 전이를 포함하는 항암 작용 효과를 나타낸다. 또한, AMPK 활성화는 우수한 혈당 강하 작용과 지질 저하 작용을 나타내어 당뇨, 비만, 고지혈증, 고콜레스테롤혈증, 지방간, 관상동맥질환, 골다공증, 다낭성 난소증후군 및 대사성 증후군 등의 치료를 위해 유용하게 이용될 수 있다. [화학식 1] The present invention provides an N1-ring amine-N2-substituted biaguanide derivative represented by the following formula (1), a pharmaceutically acceptable salt thereof, a process for producing the same, and a pharmaceutical composition containing the same. The biguanide derivatives of the present invention exhibit an excellent activating effect of AMPK which is involved in the regulation of energy metabolism even at a small dose compared to conventional drugs, and thus exhibit an anticancer effect including cancer cell proliferation inhibition effect and cancer recurrence and metastasis. In addition, AMPK activation exhibits excellent hypoglycemic action and lipid lowering action and can be useful for the treatment of diabetes, obesity, hyperlipidemia, hypercholesterolemia, fatty liver, coronary artery disease, osteoporosis, polycystic ovary syndrome and metabolic syndrome . [Chemical Formula 1]

Method of preparing n-carbamoylethyloxanylate

Process for the preparation of aminoguanidine derivatives

1-Phenylaminoguanidine derivs, of formula(I)[R1R2, R3=H, halo, alkyl, NO2, CF3, alkoxy; R4,R5=alkyl or together 5-8 membered satd. hetenocycle contg. another N or O atom and (Un)substd. by 1 or 2 Me, CH2OH and/or HOCH2CH2; R6,R7=H, alkyl, alkenyl are prepd. Thus, a mixt. of 2-MeC6H4NHNH2,HCl, anhydn. PrOH, and N:CNMe2 is stirred at 130≰C and under N2 for 5hr to give 63.4% 1-(2-methylphenyl)-4, 4- dimethyl-aminoguanidine. HCl. (I) have antiarrhythmic and caridoprotectant activity and also are active against cardiac flicker.

Method of producing aminoguanidine derivatives or acid-additive salts thereof

The invention relates to new aminoguanidine derivatives of the general formula (I), <IMAGE> I wherein R1, R2 and R3 each represent hydrogen or halogen atom, C1-4 alkyl, nitro, trifluoromethyl or C1-4 alkoxy group, R4 and R5 represent a C1-4 alkyl group, furthermore NR4R5 may form a 5 to 7 membered saturated heterocyclic group containing either one or two nitrogen atoms or a nitrogen and an oxygen atom and being optionally substituted by one or two methyl, hydroxymethyl or hydroxyethyl groups, R6 and R7 each represent a hydrogen atom, normal or branched C1-4 alkyl or C2-4 alkenyl group, and to their pharmaceutically acceptable acid addition salts as well as to a process for the preparation thereof. The new compounds of the invention possess valuable antiarrhythmic activity and are devoid of the undesired circulatory side effects of the known antiarrhythmic compounds.

Method for preparing aryl isothiourea

本发明公开了一种制备芳基异硫脲的方法，将氢化物悬于溶剂中，然后依次加入硫脲、邻二碘苯，接着反应，制备芳基异硫脲。异硫脲结构广泛存在于一些活性的天然产物、化学药物及反应催化剂中，是重要的化学合成砌块。现有合成需要过渡金属介导，存在条件苛刻、金属催化剂污染等问题。本发明以氢化钠作用于邻二碘苯，与硫脲进行S‑芳基化合成S‑（2‑碘芳基）异硫脲，该方法操作简单，底物范围广泛，且邻位取代的二碘苯具有高度的区域选择性，尤其是，本发明公开的方法在5小时内的反应时间下，能够取得优异的收率。

HERBICID12

Compounds and methods of treating cancer

Presented herein inter alia are novel compounds and methods of using the same for the treatment of cancers.

Sulfonamide compounds as protease inhibitors

The present invention relates to cysteine protease inhibitors of the general formula I, the pharmaceutically acceptable salts and N-oxides thereof; their uses as therapeutic agents and the methods of their making.

Method for preparing phenacetylguanidines

Method of producing derivatives of aminoguanidine or their acid-additive salts

The invention relates to new aminoguanidine derivatives of the general formula (I), <IMAGE> I wherein R1, R2 and R3 each represent hydrogen or halogen atom, C1-4 alkyl, nitro, trifluoromethyl or C1-4 alkoxy group, R4 and R5 represent a C1-4 alkyl group, furthermore NR4R5 may form a 5 to 7 membered saturated heterocyclic group containing either one or two nitrogen atoms or a nitrogen and an oxygen atom and being optionally substituted by one or two methyl, hydroxymethyl or hydroxyethyl groups, R6 and R7 each represent a hydrogen atom, normal or branched C1-4 alkyl or C2-4 alkenyl group, and to their pharmaceutically acceptable acid addition salts as well as to a process for the preparation thereof. The new compounds of the invention possess valuable antiarrhythmic activity and are devoid of the undesired circulatory side effects of the known antiarrhythmic compounds.

Patent SU401047A3

Novel aminoguanidine derivative and manufacture

(57)【要約】本公報は電子出願前の出願データであるた め要約のデータは記録されません。

Method of preparing phenoxypropylamine derivatives or salts thereof

Method of producing derivatives of carbamide

СПОСОБ ПОЛУЧЕНИЯ ПРОИЗВОДНЫХ МОЧЕВИНЫ общей формулы 1 RI-NH-CO-NC где R, - алкил С - С, фенил, который может быть замещен одним или двум  атомами хлора или трифенильной . группой, бензил, циклогексил; R - диклогексил, алкил С фенил , который может быть замещен метоксигруппой, трифторметильной группой, с ис лы П где и ор ли цель щей стви Н-ка форм где в пр зу  или атомом хлора, нитрргруппой, бензил, алкилен С,, карбэтоксиметил, гидроксиэтил , пиридил; алкил С .; водород, вместе с соседним атомом азота могут образовьшать морфолин, тетрагидроизохинолин , бензтиазолилгруппы пользованием амина общей формуНи RJ имеют указанные значени , ганического растворител , о тчающийс  тем, что, с ю упрощени  процесса,амин обформулы П подвергают взаимодейю с сульфимидным пf oизвoдным рбамоилбензойной кислоты общей улы III R-NH -СО -N Rj имеет указанные значени , исутствии триэтиламина, испольв качестве растворител  ацетон смесь вода-ацетон. METHOD FOR OBTAINING UREA DERIVATIVES of general formula 1 RI-NH-CO-NC where R is C-C alkyl, phenyl, which can be substituted by one or two chlorine atoms or triphenyl. group, benzyl, cyclohexyl; R is diclohexyl, alkyl C is phenyl, which can be substituted by a methoxy group, a trifluoromethyl group, from the use of P, where it is the goal of the H-ka form, where it can be either blunt or chlorine atom, nitrgroup, benzyl, alkylene C, carbethoxymethyl, hydroxyethyl, pyridyl; alkyl s .; hydrogen, together with the adjacent nitrogen atom, can form morpholine, tetrahydroisoquinoline, benzthiazolyl groups using the amine of the general formNi RJ have the indicated meanings, a ganic solvent, due to the fact that, to simplify the process, the amine of the formula P undergoes an interaction with the reference structure, it is aspidible, it is aspidible, and the heart can not be at the same wavelength, but the heart will not be at the same wavelength, you will need to go to the heart, and you will not have any at any time, you will not have any way to go ...

N1-cyclic amine-n5-substituted biguanide derivatives, methods of preparing the same and pharmaceutical composition comprising the same

본 발명은 하기 화학식 1로 표시되는 N1-고리아민-N5-치환된 바이구아나이드 유도체 또는 그의 약학적으로 허용가능한 염, 이의 제조방법 및 이를 유효성분으로 하는 약학 조성물을 제공한다. 본 발명의 바이구아나이드 유도체는 기존 약물에 비해 적은 복용량으로도 에너지 대사 조절에 관여하는 AMPK가 우수한 활성화 효과를 나타냄으로써, 암세포 증식 억제 효과 및 암의 재발과 전이를 포함하는 항암 작용 효과를 나타낸다. 또한, AMPK 활성화는 우수한 혈당 강하 작용과 지질 저하 작용을 나타내어 당뇨, 비만, 고지혈증, 고콜레스테롤혈증, 지방간, 관상동맥질환, 골다공증, 다낭성 난소증후군 및 대사성 증후군 등의 치료를 위해 유용하게 이용될 수 있다. [화학식 1] The present invention provides a N1-ring amine-N5-substituted bi-guanidine derivative represented by the following formula (1), a pharmaceutically acceptable salt thereof, a process for producing the same, and a pharmaceutical composition containing the same. The biguanide derivatives of the present invention exhibit an excellent activating effect of AMPK which is involved in the regulation of energy metabolism even at a small dose compared to conventional drugs, and thus exhibit an anticancer effect including cancer cell proliferation inhibition effect and cancer recurrence and metastasis. In addition, AMPK activation exhibits excellent hypoglycemic action and lipid lowering action and can be useful for the treatment of diabetes, obesity, hyperlipidemia, hypercholesterolemia, fatty liver, coronary artery disease, osteoporosis, polycystic ovary syndrome and metabolic syndrome . [Chemical Formula 1]

COPOLYMERS, POLYMERIC PARTICLES CONTAINING THE Mentioned COPOLYMERS, AND POLYMERIC BINDERS FOR COMPOSITIONS OF RADIATION-SENSITIVE COATINGS FOR NEGATIVE COPY RADIATIVE FILMS

1. Сополимер, содержащий:- мономерные звенья А, имеющие цианосодержащую боковую группу, в которых цианогруппа не присоединена непосредственно к основной цепи сополимера;- мономерные звенья В, имеющие пленкообразующую боковую группу;- мономерные звенья С, имеющие боковую цепь, содержащую поли(этиленгликоль), поли(пропиленгликоль) и/или статистический поли(этиленгликоль-пропиленгликоль), при этом упомянутая боковая цепь присоединена к основной цепи сополимера через амидный, карбаматный, сложноэфирный линкер или линкер мочевины; и- необязательно мономерные звенья D, имеющие, по меньшей мере, одну функциональную группу, способную претерпевать реакцию сшивания в результате проведения катионной полимеризации.2. Сополимер по п.1, описывающийся формулойФормула 1где:- а, с и d представляют собой молярные доли, варьирующиеся в диапазоне от приблизительно 0,01 до приблизительно 0,90;- b и е представляют собой молярные доли, варьирующиеся в диапазоне от приблизительно 0 до приблизительно 0,90;- А1 представляет собой мономерные звенья А;- А2 представляет собой мономерные звенья А или мономерные звенья В;- А3 представляет собой мономерные звенья С;- А4 представляет собой мономерные звенья В; и- А5 представляет собой мономерные звенья В или мономерные звенья D,где мономерные звенья А в А1 и А2 отличаются друг от друга, и где мономерные звенья В в А2, А4 и А5 отличаются друг от друга.3. Сополимер по п.1, где мономерные звенья А описываются формулойгде:- R представляет собой водород, метил или этил;- Rотсутствует или представляет собой от одного до четырех алкильных или алкилокси-заместителей, при этом алкильные и алкилокси-заместители необязател� РОССИЙСКАЯ ФЕДЕРАЦИЯ (19) RU (11) (13) 2012 102 774 A (51) МПК C08F 220/36 (2006.01) ФЕДЕРАЛЬНАЯ СЛУЖБА ПО ИНТЕЛЛЕКТУАЛЬНОЙ СОБСТВЕННОСТИ (12) ЗАЯВКА НА ИЗОБРЕТЕНИЕ (21)(22) Заявка: 2012102774/04, 14.09.2010 (71) Заявитель(и): МАЙЛАН ГРУП (VN) Приоритет(ы): (30) Конвенционный приоритет: 15.09.2009 US 61/242,421 R U (43) Дата публикации ...

Copolymers, polymeric particles comprising said copolymers and copolymeric binders for radiation-sensitive coating compositions for negative-working radiation-sensitive lithographic printing plates

코폴리머, 및 상기 코폴리머를 포함하는 폴리머성 입자, 폴리머성 입자의 제조 방법, 코폴리머성 결합제, 코폴리머성 결합제의 제조 방법, 근적외선 감응성 코팅 조성물, 네거티브형 평판 오프셋 인쇄판, 네거티브형 평판 오프셋 인쇄판의 제조 방법, 및 상기 판의 이미징 방법 및 상기 이미징된 판에 의해 인쇄하는 방법이 제공된다. Polymeric particles comprising the copolymer, a method of producing polymeric particles, a copolymeric binder, a method of producing a copolymeric binder, a near-infrared sensitive coating composition, a negative plate offset printing plate, a negative plate offset printing plate And an imaging method of the plate and a method of printing by the imaged plate are provided.

Process for preparing derivatives of thiocarbamoyl guanidine

A method of combatting weeds comprising applying to the soil pre- emergence and/or post-emergence of said weeds at a dosage rate of from 1 to 6 kg/ha one or more herbicide compounds having the general formula <IMAGE> in which: each R represents a phenyl group which may be substituted by one or more substituents selected from halogen atoms, an alkyl group having one to three carbon atoms and a haloalkyl group having 1 to 3 carbon atoms, R<1> and R<2> independently represent an alkyl group having 1 to 3 carbon atoms, and alkoxyl group having 1 to 3 carbon atoms or R<1> and R<2> together form an alkylidenic chain of 4 or 5 carbon atoms which may be interrupted by a heteroatom, and n is 1 or 2. Many of the compounds of formulae (I) and (II) are new. The compounds may be prepared by the following reactions: <IMAGE>

Biguanide compounds and use thereof

본 발명은 구아니딘 화합물 및 이의 용도에 관한 것으로서, 더욱 자세하게는 암세포 증식 억제, 암 전이와 암 재발을 억제에 우수한 효과를 나타내는 구아니딘 유도체, 이의 제조 방법 및 이를 유효 성분으로 함유하는 약학 조성물에 관한 것이다. 본 발명에 따른 구아니딘 유도체는 기존 약물에 비해 적은 복용량으로도 우수한 암 세포 증식 억제 및 암 전이와 재발 억제 효과를 나타내며, 따라서 자궁암, 유방암, 위암, 뇌암, 직장암, 대장암, 폐암, 피부암, 혈액암 및 간암 등의 다양한 암의 치료, 암세포의 증식 억제, 및 암전이 억제에 유용하게 이용될 수 있다. The present invention relates to a guanidine compound and its use, and more particularly, to a guanidine derivative exhibiting excellent effects on inhibiting cancer cell proliferation, cancer metastasis and cancer recurrence, a method for preparing the same, and a pharmaceutical composition containing the same as an active ingredient. The guanidine derivative according to the present invention exhibits excellent cancer cell proliferation inhibition and cancer metastasis and recurrence inhibitory effects even at a small dose compared to conventional drugs, and thus uterine cancer, breast cancer, stomach cancer, brain cancer, rectal cancer, colon cancer, lung cancer, skin cancer, blood cancer And it can be usefully used in the treatment of various cancers such as liver cancer, inhibition of proliferation of cancer cells, and inhibition of cancer metastasis.

Biguanide compounds and their use

Method for controlling weed plants

A method of combatting weeds comprising applying to the soil pre- emergence and/or post-emergence of said weeds at a dosage rate of from 1 to 6 kg/ha one or more herbicide compounds having the general formula <IMAGE> in which: each R represents a phenyl group which may be substituted by one or more substituents selected from halogen atoms, an alkyl group having one to three carbon atoms and a haloalkyl group having 1 to 3 carbon atoms, R<1> and R<2> independently represent an alkyl group having 1 to 3 carbon atoms, and alkoxyl group having 1 to 3 carbon atoms or R<1> and R<2> together form an alkylidenic chain of 4 or 5 carbon atoms which may be interrupted by a heteroatom, and n is 1 or 2. Many of the compounds of formulae (I) and (II) are new. The compounds may be prepared by the following reactions: <IMAGE>

Method of fighting weeds

Azo mediators

본 발명은 아조 화합물에 관한 것이며, 진단 방법에서 매개체로서의 이의 용도에 관한 것이다. 또한, 본 발명은 이러한 아조 화합물을 포함하는 검출 시약, 키트 및 시험 요소에 관한 것이다. The present invention relates to azo compounds and to their use as mediators in diagnostic methods. The present invention also relates to detection reagents, kits and test elements comprising such azo compounds.

CYTOFECTINE DERIVED FROM PIPERAZINE

Latent acids and their use

The invention pertains to a compound generating an acid of the formula (I) or (II), for instance corresponding sulfonium and iodonium salts, as well as corresponding sulfonyloximes, Formula (I) and Formula (II), wherein X is CH 2 or CO; Y is O, NR 4 , S, O(CO), O(CO)O, O(CO)NR 4 , OSO 2 , O(CS), or O(CS)NR 4 ; R 1 is for example C 1 -C 18 alkyl, C 1 -C 10 haloalkyl, C 2 -C 12 alkenyl, C 4 -C 30 cycloalkenyl, phenyl-C 1 -C 3 -alkyl, C 3 -C 30 cycloalkyl, C 3 -C 30 cycloalkyl-C 1 -C 18 alkyl, interrupted C 2 -C 18 alkyl, interrupted C 3 -C 30 cycloalkyl, interrupted C 3 -C 30 cycloalkyl-C 1 -C 18 alkyl, interrupted C 4 -C 30 cycloalkenyl, phenyl, naphthyl, anthracyl, phenanthryl, biphenylyl, fluorenyl or heteroaryl, all unsubstituted or are substituted; or R 1 is NR 12 R 13 ; R 2 and R 3 are for example C 3 -C 30 cycloalkylene, C 3 -C 30 cycloalkyl-C 1 -C 18 alkylene, C 1 -C 18 alkylene, C 1 -C 10 haloalkylene, C 2 -C 12 alkenylene, C 4 -C 30 cycloalkenylene, phenylene, naphthylene, anthracylene, phenanthrylene, biphenylene or heteroarylene; all unsubstituted or substituted; R 4 is for example C 3 -C 30 cycloalkyl, C 3 -C 30 cycloalkyl-C 1 -C 18 alkyl, C 1 -C 18 alkyl, C 1 -C 10 haloalkyl, C 2 -C 12 alkenyl, C 4 -C 30 cycloalkenyl, phenyl-C 1 -C 3 -alkyl; R 12 and R 13 are for example C 3 -C 30 cycloalkyl, C 3 -C 30 cycloalkyl-C 1 -C 18 alkyl, C 1 -C 18 alkyl, C 1 -C 10 haloalkyl, C 2 -C 12 alkenyl, C 4 -C 30 cycloalkenyl, phenyl-C 1 -C 3 -alkyl, Ar, (CO)R 15 , (CO)OR 15 or SO 2 R 15 ; and Ar is phenyl, biphenylyl, fluorenyl, naphthyl, anthracyl, phenanthryl or heteroaryl, all unsubstituted or substituted.

BIGUANID DERIVATIVES

ÐÎÑÑÈÉÑÊÀß ÔÅÄÅÐÀÖÈß (19) RU (51) ÌÏÊ 7 (11) 2003 130 070 (13) A C 07 D 207/04 ÔÅÄÅÐÀËÜÍÀß ÑËÓÆÁÀ ÏÎ ÈÍÒÅËËÅÊÒÓÀËÜÍÎÉ ÑÎÁÑÒÂÅÍÍÎÑÒÈ, ÏÀÒÅÍÒÀÌ È ÒÎÂÀÐÍÛÌ ÇÍÀÊÀÌ (12) ÇÀßÂÊÀ ÍÀ ÈÇÎÁÐÅÒÅÍÈÅ (21), (22) Çà âêà: 2003130070/04, 20.03.2002 (71) Çà âèòåëü(è): ÌÅÐÊ ÏÀÒÅÍÒ ÃÌÁÕ (DE) (30) Ïðèîðèòåò: 21.03.2001 FR 0103846 (43) Äàòà ïóáëèêàöèè çà âêè: 10.04.2005 Áþë. ¹ 10 (74) Ïàòåíòíûé ïîâåðåííûé: Âåñåëèöêà Èðèíà Àëåêñàíäðîâíà (86) Çà âêà PCT: EP 02/03119 (20.03.2002) Àäðåñ äë ïåðåïèñêè: 101000, Ìîñêâà, Ì.Çëàòîóñòèíñêèé ïåð., ä.10, êâ.15, "ÅÂÐÎÌÀÐÊÏÀÒ", È.À.Âåñåëèöêîé (54) ÏÐÎÈÇÂÎÄÍÛÅ ÁÈÃÓÀÍÈÄÀ R U â êîòîðîé: R1 è R2, êîòîðûå ìîãóò áûòü îäèíàêîâûìè èëè ðàçëè÷íûìè, îáîçíà÷àþò ðàçâåòâëåííóþ èëè íåðàçâåòâëåííóþ (Ñ1-Ñ6)àëêèëüíóþ öåïü, èëè R1 è R2 âìåñòå îáðàçóþò 3-8-÷ëåííîå êîëüöî, âêëþ÷àþùåå àòîì àçîòà, ê êîòîðîìó îíè ïðèñîåäèíåíû, R3 è R4 âìåñòå îáðàçóþò êîëüöî, âûáðàííîå èç ãðóïïû àçèðèäèíà, ïèððîëèëà, èìèäàçîëèëà, ïèðàçîëèëà, èíäîëèëà, èíäîëèíèëà, ïèððîëèäèíèëà, ïèïåðàçèíèëà è ïèïåðèäèëà, âêëþ÷àþùåå àòîì àçîòà, ê êîòîðîìó îíè ïðèñîåäèíåíû, à òàêæå òàóòîìåðíûå, ýíàíòèîìåðíûå, äèàñòåðåîèçîìåðíûå è ýïèìåðíûå ôîðìû, ñîëüâàòû è ôàðìàöåâòè÷åñêè ïðèåìëåìûå ñîëè. 2. Ñîåäèíåíè ïî ï.1, äë êîòîðûõ R1 è R2, êîòîðûå ìîãóò áûòü îäèíàêîâûìè èëè ðàçëè÷íûìè, îáîçíà÷àþò (Ñ1-Ñ6)àëêèëüíóþ öåïü. 3. Ñîåäèíåíè ïî ï.2, äë êîòîðûõ Rl è R2, êîòîðûå ìîãóò áûòü îäèíàêîâûìè èëè ðàçëè÷íûìè, îáîçíà÷àþò ðàäèêàë, âûáðàííûé èç ãðóïïû ðàäèêàëîâ, êîòîðà âêëþ÷àåò ìåòèë, ýòèë, ïðîïèë, èçîïðîïèë, áóòèë, âòîð-áóòèë, òðåò-áóòèë, ïåíòèë è ãåêñèë. 4. Ñîåäèíåíè ïî ï.3, äë êîòîðûõ R1 è R2 îáîçíà÷àþò ìåòàëüíûé ðàäèêàë. 5. Ñîåäèíåíè ïî îäíîìó èç ï.ï.1-4, äë êîòîðûõ R3 è R4 âìåñòå îáðàçóþò Ñòðàíèöà: 1 RU A 2 0 0 3 1 3 0 0 7 0 A Ôîðìóëà èçîáðåòåíè 1. Ñîåäèíåíè îáùåé ôîðìóëû (I) 2 0 0 3 1 3 0 0 7 0 (87) Ïóáëèêàöè PCT: WO 02/07474 (26.09.2002) R U (85) Äàòà ïåðåâîäà çà âêè PCT íà íàöèîíàëüíóþ ôàçó: 21.10.2003 (72) Àâòîð(û): Æåðàð ÌÓÀÍÅ (FR), Äàíüåëü ÊÐÀÂÎ (FR) ïèððîëèäèíèëüíîå êîëüöî. 6. Ñîåäèíåíèå ïî ï.1, êîòîðîå ïðåäñòàâë åò ...

Synthesis and use of amino acid fluorides as peptide coupling reagents

A compound of the formula ##STR1## or the acid fluoride salts thereof wherein BLK is an N-amino protecting group or hydrogen AA is an amino acid residue and X is H or a protecting group useful as a coupling agent in peptide synthesis.

Substituted benzoylcyclohexenones

FIELD: organic chemistry. SUBSTANCE: invention describes novel substituted benzoylcyclohexenones of the general formula (I): wherein values Q, Y, Z, R 1 -R 5 and their possible tautomeric forms and their possible salts given in the invention claim. Invention proposes substituted benzoylcyclohexenones of the general formula (I) that possess the herbicide activity. EFFECT: valuable property of compounds. 2 cl, 10 tbl, 6 ex ÐÎÑÑÈÉÑÊÀß ÔÅÄÅÐÀÖÈß (19) RU (11) 2 316 550 (13) C2 (51) ÌÏÊ C07D 233/32 C07D 239/10 C07D 257/04 C07D 261/02 C07D 261/04 ÔÅÄÅÐÀËÜÍÀß ÑËÓÆÁÀ C07D 261/18 ÏÎ ÈÍÒÅËËÅÊÒÓÀËÜÍÎÉ ÑÎÁÑÒÂÅÍÍÎÑÒÈ,C07D 265/02 ÏÀÒÅÍÒÀÌ È ÒÎÂÀÐÍÛÌ ÇÍÀÊÀÌ C07D 277/46 C07D 285/08 C07D 295/20 (12) (30) Êîíâåíöèîííûé ïðèîðèòåò: 16.05.2001 DE 10123887.8 (45) Îïóáëèêîâàíî: 10.02.2008 Áþë. ¹ 4 (56) Ñïèñîê äîêóìåíòîâ, öèòèðîâàííûõ â îò÷åòå î ïîèñêå: US 4780127, 25.10.1988. WO 000521 A1, 03.02.2000. RU 2045512 C1, 10.10.1995. (86) Çà âêà PCT: EP 02/04851 (03.05.2002) (73) Ïàòåíòîîáëàäàòåëü(è): Áàéåð ÊðîïÑàéåíñ Àà (DE) (87) Ïóáëèêàöè PCT: WO 02/092574 (21.11.2002) Àäðåñ äë ïåðåïèñêè: 103064, Ìîñêâà, óë. Êàçàêîâà,16, ÍÈÈÐ Êàíöåë ðè "Ïàòåíòíûå ïîâåðåííûå Êâàøíèí, Ñàïåëüíèêîâ è ïàðòíåðû", Â.Ï.Êâàøíèíó (54) ÇÀÌÅÙÅÍÍÛÅ ÁÅÍÇÎÈËÖÈÊËÎÃÅÊÑÅÍÎÍÛ (57) Ðåôåðàò: Îïèñûâàþòñ íîâûå çàìåùåííûå áåíçîèëöèêëîãåêñåíîíû îáùåé ôîðìóëû (I) â êîòîðîé Q, Y, Z, R 1-R 5 èìåþò óêàçàííûå â ôîðìóëå èçîáðåòåíè çíà÷åíè , âêëþ÷à èõ âñå âîçìîæíûå òàóòîìåðíûå ôîðìû è èõ âîçìîæíûå ñîëè. Òåõíè÷åñêèé ðåçóëüòàò - çàìåùåííûå áåíçîèëöèêëîãåêñåíîíû îáùåé ôîðìóëû (I) îáëàäàþò ãåðáèöèäíîé àêòèâíîñòüþ. 1 ç.ï. ô-ëû, 6 òàáë. Ñòðàíèöà: 1 C 2 C 2 (85) Äàòà ïåðåâîäà çà âêè PCT íà íàöèîíàëüíóþ ôàçó: 16.12.2003 (72) Àâòîð(û): ØÂÀÐÖ Õàíñ-Ãåîðã (DE), ÌÞËËÅÐ Êëàóñ-Õåëüìóò (DE), ÕÅÐÐÌÀÍÍ Øòåôàí (DE), ÕÎÉØÅÍ Äîðîòåå (DE), ÊÀÒÅÐ Êðèñòèàí (DE), ËÅÐ Øòåôàí (DE), ØÀËËÜÍÅÐ Îòòî (DE), ÄÐÅÂÅÑ Ìàðê Âèëüõåëüì (DE), ÄÀÌÅÍ Ïåòåð (DE), ÔÎÉÕÒ Äèòåð (DE), ÏÎÍÒÖÅÍ Ðîëüô (DE), ÍÀÐÀÁÓ Øèíè÷è (JP), ßÍÀÃÈ Àêèõèêî (JP), ÃÎÒÎ Òîøèî (JP), ßÌÀÃÓ×È Éîøèõèðî (JP), ...

Reversible protease inhibitors

本发明涉及新的可逆蛋白酶抑制剂。该抑制剂对半胱氨酸蛋白酶是专一的。所述抑制剂的例子包括结构式(1)的化合物。

Method of fighting weeds

Copolymers, polymer particles containing said copolymers, and copolymer bindiners for radiation-sensitive coating compositions for negative radiation-sensitive lithographic printing plates

FIELD: chemistry. SUBSTANCE: invention describes a copolymer containing monomer units A having a cyano-containing side group, monomer units B having an alkyl and an aryl film-forming side group, monomer units C having a side chain containing poly(ethylene glycol), poly(propylene glycol) and/or statistical poly(ethylene glycol-propylene glycol) and optionally monomer units D having at least one functional group capable of undergoing a crosslinking reaction via cationic polymerisation. EFFECT: copolymer is further used to produce polymer particles for use in radiation-sensitive coating compositions for negative radiation-sensitive lithographic printing plates. 11 cl, 6 dwg, 2 tbl, 26 ex РОССИЙСКАЯ ФЕДЕРАЦИЯ (19) RU (51) МПК C08F 220/36 C08F 212/10 C08F 212/14 C08F 220/10 C08F 220/54 C08F 290/06 (11) (13) 2 571 098 C2 (2006.01) (2006.01) (2006.01) (2006.01) (2006.01) (2006.01) ФЕДЕРАЛЬНАЯ СЛУЖБА ПО ИНТЕЛЛЕКТУАЛЬНОЙ СОБСТВЕННОСТИ (12) ОПИСАНИЕ (21)(22) Заявка: ИЗОБРЕТЕНИЯ К ПАТЕНТУ 2012102774/04, 14.09.2010 (24) Дата начала отсчета срока действия патента: 14.09.2010 (72) Автор(ы): НГУЙЕН Ми Т. (CA), ЛОКА Марк-Андре (CA) (73) Патентообладатель(и): МАЙЛАН ГРУП (VN) Приоритет(ы): (30) Конвенционный приоритет: (43) Дата публикации заявки: 27.09.2013 Бюл. № 27 R U 15.09.2009 US 61/242,421 (45) Опубликовано: 20.12.2015 Бюл. № 35 C 2 C 2 (85) Дата начала рассмотрения заявки PCT на национальной фазе: 22.03.2012 (86) Заявка PCT: 2 5 7 1 0 9 8 CA 2010/001400 (14.09.2010) R U 2 5 7 1 0 9 8 (56) Список документов, цитированных в отчете о поиске: Edward, J.et al "Photogenerated Base in Polymer Curing and Imaging: Cross-Linking of base-Sensitive polymer Containing Enolizable pendant Groups.Chen.Mater.1997 Vol.9p.2862". JP 62063595 A 27.03.1987. US 2008/0139737 A1 16.06.2008. GB 780284 A 31.07.1957. US 4297431 A 27.10.1981. Reghunadhan, C.P.et al "Advance in polymer Science, 155, New (см. прод.) (87) Публикация заявки PCT: WO 2010/148520 (29.12.2010) Адрес для переписки: 129090, ...

Cathepsin s inhibitors

Cathepsin S inhibitors having formula (I), (II), (III) or (IV) as shown in the specification. These inhibitors can be used to treat cancer and autoimmune/inflammatory diseases.

Method of preparing heterocyclic derivatives of guanidine or their salts

Methoximinophenylacetic acid amides

New 2-methoxyimino-2-phenyl-acetamide derivatives useful as microbicides, especially fungicides for plant protection

2-Methoxyimino-2-phenylacetamide derivatives (I) are new. 2-Methoxyimino-2-phenylacetamide derivatives of formula (I) are new: A = H, alkoxycarbonyl, Me, Et, cyclopropyl or R; R = alkylthio, haloalkylthio, optionally substituted arylthio, alkoxycarbonylthio, alkylthiocarbonyl, SY, SNR<1>R<2>, CONR<3>R<4>, CN, CH2OR<5>, PO(OR<6>)R<7> or PS(OR<6>)R<7>, or can also be alkanoyl, alkoxycarbonyl, haloalkoxycarbonyl, alkoxycarbonylcarbonyl, alkylcarbamoyl, dialkylcarbamoyl, alkylsulfonyl or optionally substituted arylsulfonyl when A is Me; R<1> = alkyl or forms an optionally substituted ring with R<2>; R<2> = alkyl or alkoxycarbonyl or forms an optionally substituted ring with R<1>; R<3> = alkyl or optionally substituted aryl or forms an optionally substituted ring with R<4>; R<4> = alkylthio, alkylsulfonyl or haloalkylthio or forms an optionally substituted ring with R<3>; R<5>, R<6> = alkyl; R<7> = alkyl, alkoxy or alkylamino; Y = a group of formula (I) minus R; G = a bond, O or S; alkanediyl, alkenediyl or alkynediyl optionally substituted by halogen, OH, alkyl, haloalkyl or cycloalkyl; or one of the following groups with the left side bonded to Z: -Q-CQ-, -CQ-Q-, -CH2-Q-, -Q-CH2-, -CQ-Q-CH2-, -CH2-Q-CQ-, -Q-CQ-CH2-, -Q-CQ-Q-CH2-, -N=N-, SOn, CH2SOn, CQ, SOnCH2, -C(R<8>)=N-O-, -C(R<8>)=N-O-CH2-, -N(R<9>)-, -CQ-N(R<9>)-, -N(R<9>)-CQ-, -Q-CQ-N(R<2>)-, -N=C(R<8>)-Q-CH2-, -CH(R<8>)-O-N=CH-, -C(R<8>)=N-N=CH-, -N(R<9>)-CQ-Q-, -CQ-N(R<9>)-CQ-Q-, -N(R<9>)-CQ-Q-CH2-, -Q-C(R<8>)=N-O-CH2-, -N(R<9>)-C(R<8>)=N-O-CH2-, -O-CH2-C(R<8>)=N-O-CH2-, -N=N-C(R<8>)=N-O-CH2-, -C(=NOR<10>)-C(R<8>)=N-O-CH2-, -C(=NOR<10>)-C(R<8>)-O-N=CH- (sic), -C(=NOR<10>)-C(R<8>)=N-N=CH-, -C(=NOR<10>)-C(R<8>)-O-N=C(CH3)- (sic), -T-Ar<1>- or ...

Process for the preparation of N-aryl-N'-(mono- or di substituted)-urea derivatives

The invention relates to a new method for the preparation of N-aryl-N'-(mono- or disubstituted)-urea derivatives having the general formula (I), ##STR1## wherein Aryl is an optionally substituted phenyl group, and R 1 and R 2 each stand for an optionally substituted alkyl, cycloalkyl, alkoxy or phenyl group, or R 1 and R 2 may form, together with the adjacent nitrogen atom, a nitrogen-containing heterocyclic group which may contain a further hetero atom, or one of R 1 and R 2 may also stand for hydrogen, with the proviso that if one of R 1 and R 2 is an optionally substituted phenyl group, the other may represent only hydrogen atom or an optionally substituted alkyl or alkoxy group, by reacting a carbamate of the general formula (II) with an amine of the general formula (III), R.sup.1 R.sup.2 N--CO--X (II) Aryl--NH.sub.2 (III) or a carbamate of the general formula (IV) with an amine of the general formula (V), Aryl--NH--CO--X (IV) R.sup.1 R.sup.2 NH (V) wherein R 1 , R 2 and Aryl are as defined above and X is a lower alkoxy, phenoxy or substituted phenoxy group, in the presence of a tertiary amine catalyst. According to the invention a tertiary alkylamine containing altogether at least 6 carbon atoms and minimum one alkyl chain with at least 4 carbon atoms or a mixture of such tertiary alkylamines is applied as catalyst.

Method of obtaining derivatives of aminopropanol

New compounds of the formula …<CHEM>… or a pharmaceutically acceptable salt thereof, in which formula… R<1> form H, a straight or branched alkyl group containing 1-5 carbon atoms, a cycloalkyl group containing 3-6 carbon atoms, or a cycloalkylalkyl group containing 4-6 carbon atoms;… R<2> is H, Cl, Br or F;… n is 2, 3, or 4;… R<1><1> and R<1><2>, which are the same or different, are H, an alkyl group containing 1-4 carbon atoms, a hydroxyalkyl group containing 1-4 carbon atoms, an alkoxyalkyl group containing 2-4 carbon atoms in total, or R<1><1> and R<1><2> together with the adjacent nitrogen atom form a morpholino group, are described, as well as methods for their preparation, pharmaceutical preparations thereof and methods of treatment employing the same. The compounds are potent beta 1-selective adrenoceptor blockers having a degree of intrinsic activity.

Rapid purification by polymer supported quench

Novel polymer-supported quenching reagents of Formula (I): P-L-Q, wherein P is a polymer of low chemical reactivity which is soluble or insoluble; Q is one or more quenching reagents, or an acid or base addition salts thereof, that are capable of selective covalent reaction with unwanted byproducts, or excess reagents; and L is one or more chemically robust linkers that join P and Q; are described, as well as methods for their preparation and methods for their use in the rapid purification of synthetic intermediates and products in organic synthesis, combinatorial chemistry and automated organic synthesis.

NOVEL ARYL PIPERAZINE-DERIVED PIPERAZIDS, METHODS FOR THEIR PREPARATION, USE THEREOF AS MEDICAMENTS AND PHARMACEUTICAL COMPOSITIONS COMPRISING SAME

Novel 5HT receptor antagonists of general formula (I) in which Ar1 and Ar2 are an aromatic residue, X is O, NH, CH2O or CH2NH, R1 is hydrogen, a linear or branched alkyl chain comprising 1-6 carbon atoms. The invention also concerns the salts, hydrates, solvates and physiologically acceptable bioprecursors for their therapeutic use, their geometric and optic isomers and their mixtures in all proportions and in racemic form. Also disclosed are methods for the preparation of these novel antagonists, their use as drugs and pharmaceutical compositions comprising them.

NEWS 3- (2-ARYL-2-PROPYL) UREES, AND THEIR USE AS HERBICIDES

L'invention concerne de nouveaux composés de formule générale : The invention relates to novel compounds of general formula:

PROCESS FOR THE PREPARATION OF ISOCYANATES BLOCKED IN THE FINALLY DIVIDED STATE

NEW AROMATIC AMINES DERIVED FROM CYCLIC AMINES USEFUL AS MEDICAMENTS

Patent FR2111960A1

New sulfonyl ureas and their preparation

N-amino carbonyl-piperazines analgesics - antiinflammatories ,hypotensives and spasmolytics

Compounds of formula (where R = alkyl or alkenyl of 1-4C straight or branched cycloaliphatic, or aromatic; R' = propyloxycarbonyl, dihydroxyethyl, or aminocarbonyl) are prepd. by treating cpds. of formula R-N=C=O with Prefd. compounds have R= CH3, C2H5, m-propyl, isopropyl, butyl, allyl, cyclohexyl or phenyl, and R' = pyrrolidinocarbonyl or isopropylaminocarbonyl. In an example, propyl isocyanate is treated with 1-(isopropylamino-carbonylmethyl) piperazine in tetrahydrofuran in the cold, and the product is converted into its maleate salt.

3-AMINO-6,7-DIALCOXY-1H-1,2,4-BENZOTHIADIAZINE-1-OXIDES 1-SUBSTITUTES AND THEIR USE AS MEDICINAL PRODUCTS

L'invention concerne des 3-amino- 1,2,4-benzothiadiazine- 1-oxydes substitués en position 1 de formule : The invention relates to 3-amino-1,2,4-benzothiadiazine-1-oxides substituted in position 1 of the formula:

Patent FR2283161B1

Patent FR2081560B1

Improvements in the preparation of substituted piperazines

4-(acyl-amino)-4'-methyl-diphenylaminesantiinflammatory

4-(Acyl-amino)-4'-methyl-diphenylamines, analgesic, antiinflammatory Improved method of preparing medicaments of formula: (where R1=H, CH3, CH3O; R2=C2H5, morpholino, C2H5O-, (CH3)2-CH=CH-, n-pentyl) in a form suitable for use.

Process for the production of naked, nu'-bis-carbamoyl-diarylaminodialcoyl esters of benzenedicarboxylic acids

NOVEL ALPHA-MERCAPTO ALKYLAMINE N-SUBSTITUTED DERIVATIVES, PROCESS FOR THE PREPARATION THEREOF, THEIR APPLICATION AS MEDICAMENTS AND THE COMPOSITIONS COMPRISING THE SAME

1/ Produits de formule (I): (CF DESSIN DANS BOPI) dans laquelle: R1 représente un atome d'hydrogène ou un radical acyle; A représente: - soit un radical alkylène ou alkénylène linéaire ou ramifié renfermant au plus 6 atomes de carbone et éventuellement substitué par un radical hydroxyle ou alcoxy renfermant au plus 6 atomes de carbone, - soit une simple liaison, R2 représente un radical cyclique comprenant 5 à 10 chaînons éventuellement substitué. X représente un atome d'oxygène ou de soufre, R3 et R4 sont tels que: ou bien R3 et R4 forment avec l'atome d'azote auxquels ils sont liés un radical cyclique comprenant 5 à 10 chaînons éventuellement substitué, ou bien R3 et R4 , identiques ou différents, représentent: - un atome d'hydrogène; - un radical hydroxyle; alcoxy, acyle ou acyloxy renfermant au plus 6 atomes de carbone; carboxy, salifié ou estérifié; cyano; - un radical alkyle, alkényle ou alkynyle linéaire ou ramifié renfermant au plus 6 atomes de carbone et éventuellement substitué; - un radical aryle ou aryloxy dans lesquels le radical aryle représente un radical cyclique comprenant 5 à 10 chaînons éventuellement substitué; (CF DESSIN DANS BOPI) leur procédé de préparation et les intermédiaires de ce procédé. Ces produits présentent d'intéressantes propriétés pharmacologiques qui justifient leur emploi à titre de médicaments. 1 / Products of formula (I): (CF DRAWING IN BOPI) in which: R1 represents a hydrogen atom or an acyl radical; A represents: - either a linear or branched alkylene or alkenylene radical containing at most 6 carbon atoms and optionally substituted by a hydroxyl or alkoxy radical containing at most 6 carbon atoms, - or a single bond, R2 represents a cyclic radical comprising 5 10-membered optionally substituted. X represents an oxygen or sulfur atom, R3 and R4 are such that: either R3 and R4 together with the nitrogen atom to which they are attached form a cyclic radical comprising 5 to 10 optionally substituted ...