ПРОИЗВОДНЫЕ 3(2Н)-ПИРИДАЗИНОНА И СПОСОБ БОРЬБЫ С ВРЕДНЫМИ НАСЕКОМЫМИ

FIELD: organic chemistry. SUBSTANCE: product of the formula (I) , where R - C 4 -C 5 -alkenyl, C 4 -alkyl, substituted OCH 3 , G-R a where G - H or R b O; R b -C 1 -C 2 -alkyl; R a - haloid-C 3 -C 8 -alkylene, dihaloid-C 3 -C 6 -alkylene, trihaloid-C 3 -C 4 -alkylene, haloid-C 3 -C 4 -alkenylene, haloid-C 6 -C 8 -cycloalkylene, haloid-C 4 -C 5 -oxacycloalkylene; A - halogen or CH 3 ; X - oxygen or sulfur atom; Y - CH 2 Q′, CH 2 CH 2 OC 6 H 4 -4Y, CH 2 CH(CH 3 )OC 5 H 4 N, (CH 2 ) 3 -C ≡ CBr, Q′-substituted phenyl, pyridyl, thienyl, naphthalene. Product is used for struggle against pests at the dose 100-500 g/ha for plant treatment, 0.1-0.5 g/kg for bait preparing and 1-10 g/m 3 for compartment treatment. Formula (I) с6б6б$ $ 0с ПЧ Го РОССИЙСКОЕ АГЕНТСТВО ПО ПАТЕНТАМ И ТОВАРНЫМ ЗНАКАМ (19) (51) МПК ВИ” 2 033 992 ' 13) СЛ С 070 237/16, 237/18, А 0л М 43/58 12) ОПИСАНИЕ ИЗОБРЕТЕНИЯ К ПАТЕНТУ РОССИЙСКОЙ ФЕДЕРАЦИИ (21), (22) Заявка: 4356230/04, 29.07.1988 (30) Приоритет: 30.07.1987 УР 62-191289; 62-319336; 63-154329 (46) Дата публикации: 30.04.1995 (56) Ссылки: Заявка ЕР 0199281, кл. С 07 0237/16, А 01М 43/56, опубл. 1986.Заявка ЕР 0183212, кл. А О1М 43/56, опубл. 1986. (71) Заявитель: Ниссан Кемикал Индастриз Лтд. (4Р) (72) Изобретатель: Такахиро Макабе[Р], Томоюки Огура[/Р], Ясуо Кавамура[/Р], Татсуо Нумата[)Р], Киминори Хирата[/Р], Масаки Кудо[4Р], Тосиро Мияке[Р], Хироси Харуяма[Р] (73) Патентообладатель: Ниссан Кемикал Индастриз Лтд. (ФР) (54) ПРОИЗВОДНЫЕ 3(2Н)-ПИРИДАЗИНОНА И СПОСОБ БОРЬБЫ С ВРЕДНЫМИ НАСЕКОМЫМИ (57) Реферат: Использование: сельское хозяйство, химические способы защиты растений. Сущность изобретения: продукт ф-лы (1), где К- С4-СБ -алкенил, Сл -алкил, замещенный ОСН С-В. где с - п, или КО; К ь-С1-С2 -алкил; К. -галоид- Сз-Сз -алкилен, дигалоид- Сз-Сб -алкилен, тригалоид- С 3-Слд -алкилен, галоид- Сз-Сд -алкенилен, галоид- Св-Сз -циклоалкилен, галоид- С 4-Сь -оксациклоалкилен, А-галоген или СН 3, Х-атом кислорода или серы, +. - СНС’, СН2СН2ОСвНа-4\, ...

Sulphur-containing derivatives of pyridazone-6 and herbicidal compositions containing the same

Novel compounds of the formula in which R is hydrogen, a cycloalkyl radical, which may be substituted, or a phenyl radical, which may be substituted, R1, R2 are alkyl radicals having 1 to 5 carbon atoms, alkenyl radicals, a phenyl or aralkyl radical, either of which may be substituted, a cycloalkyl radical, or the radical of benzohiazole, carboxymethyl, or tetrahydrofuran, are prepared by reacting the corresponding 4,5-dichloropyridazone derivatives with alkyl mercaptans, aralkyl mercaptans, thiophenols, thiocarboxylic acids or heterocycles containing thiol groups. The new compounds are useful as herbicides.ALSO:Herbicides contain compounds of the formula: in which R is hydrogen, a cycloalkyl radical which may be substituted, or a phenyl radical, which may be substituted, R1, R2 are alkyl radicals having 1 to 5 carbon atoms, alkenyl, a phenyl or aralkyl radical, either of which may be substituted, a cyclo-alkyl radical, or the radical of benzothiazole ...

FUNGICIDES

HYDRAZINOPYRIDAZINES

... 1527712 Hydrazinopyridazines SMITH KLINE & FRENCH LABORATORIES Ltd 17 Sept 1975 [18 June 1974 2 Jan 1975] 26864/74 and 20/75 Heading C2C The invention comprises compounds of the formula where two of the groups R1, R2 and R3 are H and the third is H, C 1 -C 4 alkyl, F, Cl, Br, CF 3 , OH, C 1 -C 4 alkoxy, C 2 -C 4 alkenyloxy, C 1 -C 4 alkoxycarbonyl, CN, CONH 2 , CH 2 CONH 2 , NO 2 , NH 2 , C 1 -C 4 alkanoylamino, C 1 -C 4 alkylamino or di(C 1 -C 4 alkyl)amino, R4 is H or CH 3 , R5 is isopropyl, tertiary butyl or phenylethyl. Compounds wherein R1, R2 and R3 are other than CONH 2 or alkoxycarbonyl may be prepared by reacting hydrazine or a protected derivative thereof with a compound of the formula where R11 is -CH 2 CH(OH)CH 2 NHR5, hydrogen or a phenolic protecting group, and Z is mercapto, chloro, alkoxy or phenoxy, followed if necessary by reaction with epichlorohydrin or epibromohydrin and an amine ...

Heterocyclic and phenyl compounds.

A compound of formula (i)r-s(o)nch2ch2ch=cf2, or a salt thereof, wherein n is 0, 1 or 2; and r is a group of formulae (ii)to (xxi), wherein: the s ch2ch2ch=cf2 group is at least one of r1 (when attached to a carbon atom). R2, r3, r4, r5 or r6; r1 (when attached to a ca atom)r2, r3 r4, r5 and r6 are each independently hydrogen, optionally substituted alkyl, optionally substituted alkenyl, alkynyl, cycloalkyl, alkylcycloalkyl, alkoxy, alkenyloxy, alkynyloxy, hydroxyalkyl, alkoxyalkyl, optionally substituted aryl, optionally substituted arylalkyl, optionally substituted heteroaryl, optionally substituted heteroarylalkyl, optionally substituted aryloxy, optionally substituted arylalkoxy, optionally substituted aryloxyalkyl, optionally substituted heteroaryloxy, optionally substituted heteroarylalkoxy, optionally substituted heteroaryloxyalky, haloalkyl, haloalkenyl, haloalkynyl, haloalkoxy, haloalkenyloxy, haloalkynyloxy, halogen, hydroxy, cyano, notro, -nr7r8, -nr7cor8, -nr7csr8, -nr7so2r8 ...

"Substituted nitrogen containing heterocycles as inhibitors of P38 protein kinase".

The present invention relates to inhibitors of p38, a mammalian protein kinase involved cell proliferation, cell death and response to extracellular stimuli. The invention also relates to methods for producing these inhibitors. The invention also provides pharmaceutical compositions comprising the inhibitors of the invention and methods of utilizing those compositions in the treatment and prevention of various disorders.

Heterocyclic and phenyl compounds

Substituted nitrogen containing heterocycles as inhibitors of p38 protein kinase

Substituted heteroaryl-and phenyl-sulfamoyl compounds

Pyridazinone compounds and their use as DAAO inhibitors

(4,4-Difluorobut-3-enylthio)-substituted heterocyclic or carbocyclic ring compounds having pesticidal activity

3,5-diphényl-4 (14) pyridazinones (thiones), their synthesis and their use as weedkillers.

Pyridazinone compounds and their use as DAAO inhibitors

Substituted heteroaryl-and phenyl-sulfamoyl compounds

Heterocyclic and phenyl compounds

Pyridazinone compounds and their use as DAAO inhibitors

Substituted nitrogen containing heterocycles as inhibitors of p38 protein kinase

Substituted heteroaryl-and phenyl-sulfamoyl compounds

HERBIZIDES MITTEL

MALONONITRILVERBINDUNGEN AS PESTICIDES

2-TBUTYL-4-CHLOR-5 (4-IBUTOXYMETHYLCYCLOHEXYL) - METHYLTHIO-3 (H) - PYRIDAZINON WITH INSEKTIZIDER AND AKARIZIDER ACTIVITY

PYRIDAZINON DERIVATIVES, PROCEDURES FOR ITS PRODUCTION UN YOUR USE AS FUNGICIDES.

LUBRICANT COMPOSITION WITH EXTREME-PRINTINGSUITABLE ANTI-WEAR ADDITIVES.

Procedure for the production of for example, new ISO thiourea derivatives usable as herbicide

THIONATION PROCESS USING ELEMENTARY PHOSPHORUS AND SULFUR

(4,4-DIFLUORBUT-3-ENYLTHIO) - HETEROCYCKI OR CARBOCYCLI RING SUBSTITUTED CONNECTIONS WITH PESTICIDER EFFECT

5 (BICYCLOGROUP-METHOXY/METHYLTHIO) - PYRIDAZIN-3-ONE INSECTICIDES

Arylpyridazinones as prostaglandin endoperoxide h synthase biosynthesis inhibitors

Small molecule inhibitors of the pleckstrin homology domain and methods for using same

Small molecule inhibitors of the pleckstrin homology domain and methods for using same

Pleckstrin homology domain binding compounds, pharmaceutical compositions including such compounds, and methods for their use are described herein.

PYRIDAZINONES, THEIR PREPARATION AND USE, AND MEDICAMENTS CONTAINING PYRIDAZINONES

HETEROCYCLIC ACETYLENE COMPOUNDS

PYRIDAZINONE DERIVATIVES, PREPARATION THEREOF AND INSECTICIDAL, ACARICIDAL, FUNGICIDAL COMPOSITIONS

Novel 3(2H)-pyridazinone derivatives having the formula I: (I) wherein, R is a straight or branched C2 to C6 alkyl, R1 and R2 are each independently hydrogen or a lower alkyl, R4 is a halogen, R3 is a halogen, an alkyl, a cycloalkyl, an alkoxy, a haloalkyl, a haloalkoxy, -CN, -NO2, a phenyl, a benzyloxyy, a benzyl, a phenoxy, a phenylthio, a pyridyloxy, a quinoxalyloxy, a lower alkenyloxy, a lower alkylthio, a lower haloalkylthio, Si(CH3)3, -OH, -N(CH3)2, -SCN, -COOCH3 or -OCH(CH3)COOC2H5, and n is an integer of 1 to 5, said R3 being the same or different when n is an integer of 2 to 5. A process for preparation of said derivatives is also provided. These derivatives are useful as an active ingredient of insecticidal, acaricidal, nematicidal and/or fungicidal compositions for agricultural and horticultural uses as well as of expellent compositions for ticks parasitic on animals.

PYRIDAZINONES, THEIR PREPARATION AND USE, AND MEDICAMENTS CONTAINING THEM

... 6-Aryl-3¢2H!pyridazinones of the formula I (I) wherein one of the substituents R1 or R2 denotes methoxy and the other denotes (C2-C5)alkoxy or (C3-C5)alkenyloxy and X denotes oxygen or sulfur, and their pharmacologically acceptable salts with bases, are suitable for use as a bronchospasmolytic or cardiotonic agent. Processes for the preparation of the compounds and appropriate medicaments are described.

PYRIDAZINONE DERIVATIVES, THEIR PREPARATION AND THEIR USE AS FUNGICIDES

Pyridazinone derivatives of the formula (I) where R1 is alkyl, alkenyl, cycloalkyl or unsubstituted or substituted phenyl, R2 is chlorine or bromine, R3 is hydrogen, alkyl, cycloalkyl or unsubstituted or substituted phenyl and X is SO or SO2, with the proviso that R1 is not methyl when X is SO2, R2 is chlorine and R3 is phenyl, and fungicides containing these compounds.

PYRIDAZINE DERIVATIVES AND THEIR USE AS AGRICULTURAL FUNGICIDES

PYRIDAZINONE COMPOUNDS AND THEIR USE AS DAAO INHIBITORS

The present invention provides compounds of formula (I) and pharmaceutically acceptable salts thereof, wherein R1 and R2 are as defined in the specification, processes for their preparation, pharmaceutical compositions containing them and their use in therapy.

SMALL MOLECULE INHIBITORS OF THE PLECKSTRIN HOMOLOGY DOMAIN AND METHODS FOR USING SAME

Pleckstrin homology domain binding compounds, pharmaceutical compositions including such compounds, and methods for their use are described herein.

CYCLOHEXANONE COMPOUNDS AND HERBICIDES COMPRISING THE SAME

The present invention provides a compound having an excellent efficacy for controlling weeds. A cyclohexanone compound of the formula (I): wherein m is an integer of 1, 2 or 3; n is an integer of any one of 1 to 5; X represents CH2, O, S, S(O) or S(O)2; R1 represents a hydrogen atom or a methyl group; R2 and R3 represents a hydrogen atom, a C1-6 alkyl group and the like; R4 represents a C6-10 aryl group or a five- to six- membered heteroaryl group; G represents a hydrogen atom and the like; Z represents a halogen atom, a cyano group, a nitro group, a phenyl group, a C1-6 alkyl group and the like; is useful as an active ingredient for herbicides.

THIONATION PROCESS USING ELEMENTAL PHOSPHORUS AND SULFUR

There is disclosed a novel process for preparing products of the reaction of elemental phosphorus and elemental sulfur under reaction conditions wherein the phosphorus and sulfur are combined in a pre-mix at temperatures below the reaction temperature. The pre-mix may contain a diluent which is preferably the product of the reaction. Phosphorus pentasulfide can be prepared by heating the pre-mix to reaction temperatures wherein lower exotherm temperatures and reduced vibration are observed. Organophosphorus and thionated products can be prepared by the reaction of elemental sulfur and elemental phosphorus together with an organic compound wherein the ratio of phosphorus and sulfur generally corresponding to P2S5. The process obviates the need for separately preparing phosphorus pentasulfide to prepare thionated and organophosphorus compounds.

Verfahren zur Herstellung von neuen Derivaten von Dicarbonsäurehydraziden

Verfahren zur Herstellung neuer Pyridazinderivate

Verfahren und Mittel zur Pilzbekämpfung

Verfahren zur Herstellung von neuen Derivaten von Dicarbonsäurehydraziden

Verfahren zur Herstellung von Isothioharnstoffderivaten

Verfahren zur Herstellung von neuen Pyridazinderivaten

Verfahren zur Herstellung von Mercapto-pyridazin-N-oxyden oder deren Salze

Verfahren zur Bekämpfung von Pflanzenwuchs und herbizide Mischung zur Durchführung des Verfahrens

Verfahren zur Herstellung von neuen Pyridazinderivaten

PROCEDURE FOR the PRODUCTION OF 6-HYDRAZINOPYRIDAZINEN.

PIRIDAZINONOVYE HERBICIDES

ЗАМЕЩЕННЫЕ, АЗОТСОДЕРЖАЩИЕ ГЕТЕРОЦИКЛЫ В КАЧЕСТВЕ ИНГИБИТОРОВ ПРОТЕИНКИНАЗЫ р38

... 1. Соединение формулы или его фармацевтически приемлемая соль, где каждый из Q1и Q2 независимо выбран из систем 5-6-членных ароматических карбоциклических или гетероциклических колец или систем 8-10-членных бициклических колец, состоящих из ароматических карбоциклических колец, ароматических гетероциклических колец или сочетания ароматического карбоциклического кольца и ароматического гетероциклического кольца; где Q1замещен 1-4 заместителями, которые независимо выбраны из галогена; C1-С3 -алкила, возможно замещенного NR'2, OR', CO2R' или CONR'2; O-(C1-С3)-алкила, возможно замещенного NR'2, OR', CO2R' или CONR'2; NR'2; ОСF3 ; СF3; NO2; CO2R'; CONR'; SR'; S(O2)NR'2; SСF3; CN; N(R')C(O)R4; N(R')С(O)OR4; N(R')С(О)С(O)R4; N(R')S(O2)R4; N(R')R4 ; N(R4)2; OR4; OC(O)R4; ОР(O)3Н2или N=C-NR'2, и Q2возможно замещен 1-4 заместителями, каждый из которых независимо выбран из галогена; C1-С3-линейного или разветвленного алкила, возможно замещенного NR'2, OR', CO2R', S(O2)NR'2, N=C-NR'2, R3или CONR'2; ...

PYRIDAZINONE COMPOUNDS AND THEIR USE AS DAAO INHIBITORS

СУЛЬФОНОВЫЕ СОЕДИНЕНИЯ (ВАРИАНТЫ), СОДЕРЖАЩАЯ ИХ ФАРМАЦЕВТИЧЕСКАЯ КОМПОЗИЦИЯ, СПОСОБ ИНГИБИРОВАНИЯ РАСТВОРИМОЙ ЭПОКСИДГИДРОЛАЗЫ И СПОСОБ ЛЕЧЕНИЯ ЗАБОЛЕВАНИЙ, ОПОСРЕДОВАННЫХ РАСТВОРИМОЙ ЭПОКСИДГИДРОЛАЗОЙ

В настоящем изобретении раскрываются сульфоновые соединения и композиции, которые ингибируют растворимую эпоксидгидролазу (sEH), способы получения соединений и композиций и способы лечения пациентов данными соединениями и композициями. Соединения, композиции и способы используют для лечения ряда sEH-опосредованных заболеваний, включая гипертензивные, сердечно-сосудистые, воспалительные, легочные и связанные с диабетом заболевания.

Substituted Nitrogen Containing Heterocycles as Inhibitors of p38 Protein Kinase

NEW PHENYLHYDRAZINO PYRIDAZINS SUBSTITUEES, THEIR METHOD OF PREPARATION AND THEIR APPLICATIONS

Prostaglandin endoperoksit H sentaz biyosentezi inhibitörleri olarak arilpiridazinonlar.

Thyroid hormone receptor agonists

PARP INHIBITORS

The present application disclosed compounds of Formula I wherein variables R1 and R2 are defined as described herein, which are inhibitors of PARP and provides compounds and compositions containing the compounds of Formula I. The present application further provides methods of using the disclosed PARP inhibitors for the treatment of PARP-mediated diseases and disorders.

PYRIDAZINONE COMPOUNDS AND THEIR USE AS DAAO INHIBITORS

The present invention provides compounds of formula (I) and pharmaceutically acceptable salts thereof, wherein R1 and R2 are as defined in the specification, processes for their preparation, pharmaceutical compositions containing them and their use in therapy.

PYRIDAZINONE, PREPARATION PROCESS THEREOF AND UTILISATION THEREOF, DRUGS CONTAINING PYRIDAZINONE

... 6-aryl-3 AD2H BD pyridazinone having the formula (I), wherein one of the substituents R1 or R2 represents a hydrogen and the other one (C1-C5)alcoxy, (C3-C5)alkenyloxy, (C3-C5)alkinyloxy or CF3, and wherein X is oxygen or sulfur, and pharmaceutically acceptable salts thereof with bases, are appropriate to be used as bronchospasmolytic agent. Method for the preparation of said compounds and corresponding drugs.

Pyridazinone compounds and their use as DAAO inhibitors

The present invention provides compounds of formula (I) and pharmaceutically acceptable salts thereof, wherein R1 and R2 are as defined in the specification, processes for their preparation, pharmaceutical compositions containing them and their use in therapy.

Heterocyclic neophane analogs, processes for their preparation and their use as pesticides

Compounds of the formula (I) and their stereoisomers in which A, B, C' and D independently of one another are CH or N, where at least one of the symbols A, B, C' and D must correspond to a nitrogen atom, X is CH2 or oxygen, R1 is a radical bonded to a C atom, hydrogen, trialkylsilyl, halogen, nitro, cyano, alkenyl, alkynyl, amino, cycloalkyl, phenyl, phenoxy, alkoxy, alkenyloxy, alkynyloxy, hydroxycarbonyl, alkylthio, cycloalkyloxy, alkylcarbonyl, alkoxycarbonyl, alkenyloxycarbonyl, alkynyloxycarbonyl, haloalkyl, alkoxyalkyl, haloalkoxy, haloalkylthio, haloalkoxyalkyl, alkylthioalkyl, alkoxyalkoxy, haloalkoxyalkoxy, alkenyloxyalkoxy, haloalkenyloxy, alkoxyalkylthio, alkylthioalkoxy, alkylthioalkylthio, haloalkoxycarbonyl, haloalkenyloxycarbonyl or dialkylamino, or two R1 radicals, if they are in the orthoposition to each other, together represent a methylenedioxy, ethylenedioxy or alkylene radical, R² and R3 independently of one another are alkyl, alkenyl or phenyl, or R² or R3 ...

АРОМАТИЧЕСКИЕ СОЕДИНЕНИЯ И СОДЕРЖАЩИЕ ИХ ФАРМАЦЕВТИЧЕСКИЕ КОМПОЗИЦИИ

FIELD: organic chemistry, medicine, pharmacy. SUBSTANCE: invention relates to compounds of the formula (I) where A means optionally substituted phenyl under condition that groups -CH(R 3 )N(R 2 )M-R 1 and -OD are in 1,2-position with respect to with each other in carbon ring atoms and carbon ring atom locating in ortho-position to -OD-binding group (therefore, at 3-position with respect to -CHR 3 NR 2 -binding group) is unsubstituted; B means pyridyl or pyridazinyl; R 1 is located in ring B in 1,4-position with respect to -CHR 3 NR 2 - binding group and presented as determined in claim 1 of the invention claim; R 2 means C 1-6 -alkyl; R 3 means hydrogen atom; D means hydrogen atom, optionally substituted 5-7-membered carbocyclic ring containing one double bond or D means group of the formula (CH 2 ) n CH(R 4 )C(R 5 )=C(R 6 )R 7 where R 4 means hydrogen atom, methyl or ethyl group; R 5 means hydrogen atom, methyl group, bromine, chlorine or fluorine atom; R 6 means hydrogen atom, C 1-4 -alkyl; R 7 means hydrogen atom, C 1-4 -alkyl, bromine, chlorine or fluorine atom; n = 0 or 1. Invention relates also to their pharmaceutically acceptable salts or esters hydrolyzed in vivo. Compounds are antagonists of effect of prostaglandin E-type enhancing pain. Also, invention relates to pharmaceutical composition used for pain relief based on the above described compounds and to method of pain relief using the above described compounds. Also, invention proposes method of synthesis of compounds of the formula (I) based on the above described compounds and their pharmaceutically acceptable salts or esters hydrolyzed in vivo and intermediate compounds synthesized in the process of their synthesis. EFFECT: improved methods of synthesis and preparing, valuable medicinal properties. 13 cl, 6 tbl, 67 ex 143 з6гс ПЧ сэ РОССИЙСКОЕ АГЕНТСТВО ПО ПАТЕНТАМ И ТОВАРНЫМ ЗНАКАМ (19) ВИ "” 2 498 878 ' (51) МПК? 13) С2 С 070 237/24, 213/80, 403/04, 401/04, 443/12, 417/12, А б1 К 31/455, 31/465, 31/ ...

ПРОИЗВОДНЫЕ ПИРИДАЗИНА, СПОСОБЫ ИХ ПРИМЕНЕНИЯ И ИХ ПОЛУЧЕНИЯ В КАЧЕСТВЕ ФУНГИЦИДОВ

... 1. Соединение формулы I ! ! в которой R1 и R4 независимо друг от друга обозначают гидроксигруппу, галоген, C1-С6алкоксигруппу, C1-С6галогеналкоксигруппу, C1-С6алкилтиогруппу, C1-С6галогеналкилтиогруппу, C1-С6алкиламиногруппу, C1-С6диалкиламиногруппу или цианогруппу; и ! R2 и R3 независимо друг от друга обозначают необязательно замещенный арил или гетероарил; ! или его агрохимически приемлемая соль; ! при условии, что ! если R1 и R4 оба обозначают гидроксигруппу или хлор и R3 обозначает фенил, то R2 не обозначает фенил, ! если R1 и R4 оба обозначают гидроксигруппу или хлор и R3 обозначает 4-хлорфенил, то R2 не обозначает 4-хлорфенил или пиридин-4-ил, и ! если R1 и R4 оба обозначают фтор и R3 обозначает пентафторфенил, то R2 не обозначает пентафторфенил. ! 2. Соединение по п.1, в котором R1 обозначает гидроксигруппу, галоген, C1-С6алкоксигруппу, C1-С6галогеналкоксигруппу, C1-С6алкилтиогруппу, С1-С6алкиламиногруппу или цианогруппу. ! 3. Соединение по п.1, в котором R2 обозначает необязательно ...

Способ получения 3,5-дифенил-4(1н) пиридазинонов (тионов)

3,6-disubstituted pyridazine derivatives and a process for their preparation

The invention comprises compounds of general formula: <FORM:0959534/C2/1> wherein Z represents a chlorine or bromine atom, Y represents a methylene group, an ethylene group or a methylene group substituted by a methyl group, and R and R1 each represent a hydrogen atom, an alkyl group having 1 to 4 carbon atoms or an allyl group; and their preparation by reacting a compound of formula: <FORM:0959534/C2/2> with a compound of formula: <FORM:0959534/C2/3> in which Me represents an alkali metal ion or the equivalent of an alkaline-earth metal ion which may be prepared in situ either by reacting the corresponding mercapto compound with the appropriate metal hydroxide or carbonate or by reacting 3, 6-dichloropyridazine with sodium sulphide. Pharmaceutical compositions comprise compounds I together with an inert solid or liquid carrier, and are choleretically active. Oral administration (e.g. as tablets, coated pills or syrups) is mentioned.

CEPHALOSPORIN DERIVATIVES

A new hydrazine compound and a process for making it

The invention comprises 3 : 6-dihydrazinopyridazine and salts thereof, together with a process for their preparation by reacting 3 : 6-dimercaptopyridazine with hydrazine and, if desired, converting the product into a salt. The products are pharmaceutically useful for reducing the blood pressure. In an example, 3 : 6-dimercaptopyridazine is refluxed with hydrazine hydrate in ethanol, and the product is converted to its acid sulphate or its mononitrate. Other acids specified for the formation of salts are hydrohalic acids, phosphoric, thiocyanic, acetic, propionic, oxalic, malonic and succinic acids, hydroxyethane-, benzene- and toluene-sulphonic acids, and therapeutically active acids. Starting material. 3 : 6-Dimercaptopyridazine is prepared by heating 3 : 6-dihydroxypyridazine with POCl3 and reacting the resulting 3 : 6-dichlorpyridazine with potassium sulphide (e.g. by heating in a bomb tube in ethanolic solution).

Heterocyclic derivatives

DIHYDROPYRIDAZINONE AND PYRIDAZINONE AS FUNGICIDES

SULPHONYL PYRIDAZINON DERIVATIVES FOR USE AS ALDOSE REDUKTASE INHIBITORS

NEW SULPHONYL (THIO) UREA, PROCEDURES FOR THEIR PRODUCTION AND THEIR USE AS HERBICIDES AND/OR GROWTH MODULATORS.

PYRIDAZINON DERIVATIVES, PROCEDURES FOR YOUR PRODUCTION AND YOUR USE AS FUNGICIDES.

HERBICIDE MEANS

CEPHALOSPORINDERIVATE.

HETERO-CYCLIC ONE NEOPHANANALOGA, PROCEDURES FOR YOUR PRODUCTION AND YOUR USE AS PESTICIDES.

OXIMETHER DERIVATIVES, PROCEDURES FOR YOUR PRODUCTION AND THIS CONTAINING FUNGICIDES.

Procedure for the production of new Pyridazinderivaten

SUBSTITUTED PYRIDAZINONES AS INHIBITORS OF P38

Substituted nitrogen containing heterocycles as inhibitors of p38 protein kinase

DIMERCAPTOPYRIDAZINE THIONES FOR USE IN TREATING FUNGAL INFECTIONS

DIMERCAPTOPYRIDAZINE THIONES

ANTIHYPERTENSIVE PYRIDAZIN (2H)-3-ONES

Compounds of the formula are useful antihypertensive agents.

FUNGICIDES

PP. 34001 FUNGICIDES ABSTRACT Compounds of formula (I): (I) and stereoisomers thereof, wherein X, Y and Z, which are the same or different, are hydrogen, halogen, hydroxy, optionally substituted alkyl, optionally substituted alkenyl, optionally substituted aryl, optionally substituted alkynyl, optionally substituted alkoxy, optionally substituted aryloxy, optionally substituted aralkyl, optionally substituted arylalkoxy, optionally substituted aryloxyalkyl, optionally substituted acyloxy, optionally substituted amino, acylamino, nitro, cyano, -CO2R1, -CONR2R3, or -COR4, or X and Y, when they are in adjacent positions on the phenyl ring, join to form a fused ring, either aromatic or aliphatic, optionally containing one or more heteroatoms; W is a C-linked optionally substituted six membered heterocyclic ring other than pyrimidinyl, containing two to four nitrogen atoms, and wherein adjacent substituents may together form a fused aromatic or hetero-aromatic ring; A is oxygen or sulphur; and R1, R2, R3 and R4, which are the same or different, are hydrogen, alkyl, cycloalkyl, cycloalkylalkyl, alkenyl, alkynyl, optionally substituted aryl or optionally substituted aralkyl; or metal complexes thereof. The compounds are useful fungicides.

PYRIDAZINONE DERIVATIVES AND COMPOSITIONS FOR CONTROLLING AND/OR PREVENTING INSECT PESTS

A novel 3(2H)-pyridazinone derivative of the formula ¢I!: ¢ I ! wherein, R represents an alkenyl group having 2 to 16 carbon atoms, an alkynyl group having 2 to 16 carbon atoms, an alkyl group having 3 to 8 carbon atoms substituted by an alkoxy group having 1 to 6 carbon atoms or G-Ra-; A represents hydrogen atom, halogen atom, an alkyl group having 1 to 4 carbon atoms, an alkoxy group having 1 to 4 carbon atoms, an alkylthio group having 1 to 4 carbon atoms, an alkylsulfinyl group having 1 to 4 carbon atoms or an alkylsulfonyl group having 1 to 4 carbon atoms; R1 represents hydrogen atom, halogen atom, an alkoxy group having 1 to 4 carbon atoms or hydroxyl group; X represents oxygen or sulfur atom; J represents , , , , , , , , , , , , , , , or ; as well as insecticidal, acaricidal and nematicidal compositions and compositions for expelling ticks parasitic on animals, said compositions containing ...

PYRIDAZINONES, THEIR PREPARATION AND USE, AND MEDICAMENTS CONTAINING THEM

PYRIDAZINONE DERIVATIVES

Pyridazinone derivatives represented by general formula (1); medicinally acceptable salts of them; and drug compositions containing the same as the active ingredient, wherein R1 is optionally substituted phenyl or an aromatic heterocyclic group; R2 is optionally substituted alkyl, phenyl, aralkyl, an aromatic heterocyclic group, amino, cyclic amino, cyano, carboxyl or the like; R3 is hydrogen, optionally substituted alkyl, phenyl or an aromatic heterocyclic group; and R4 is cyano, carbonyl or the like.

ROR GAMMA (RORY) MODULATORS

The present invention relates to novel compounds according to Formula (I) or a pharmaceutically acceptable salt thereof ...

AROMATIC COMPOUNDS AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM

The invention relates to compounds of formula (I), wherein A is an optionally substituted, ring system provided that the -CH(R3)N(R2)B-R1 and -OD groups are positioned in a 1,2 relationship to one another on ring carbon atoms and the ring atom positioned ortho to the -OD linking group (and therefore in the 3position relative to the -CHR3NR2- linking group) is not substituted; B is an optionally substituted ring system; R1 is positioned on ring B in a 1,3 or 1,4 relationship with the -CH(R3)N(R2)- linking group and is as defined in the description; R2 is hydrogen, C1-6alkyl, optionally substituted by hydroxy, cyano or trifluoromethyl, C2-6alkenyl (provided the double bond is not in the 1-position), (C2-6alkynyl (provided the triple bond is not in the 1-position), phenylC1-3alkyl or pyridylC1-3alkyl; R3 is hydrogen, methyl or ethyl; D is hydrogen, an optionally substituted 5-7 membered carbocyclic ring containing one double bond, C1-3alkyl substituted by an optionally substituted 5-7 membered ...

NOVEL PYRIDAZINE DERIVATIVES AND DRUGS CONTAINING THE SAME AS THE ACTIVE INGREDIENT

Pyridazine derivatives represented by general formula (1) or salts thereof; and drugs containing the same as the active ingredient: wherein R1 is (substituted) aryl; R2 is phenyl substituted with lower alkoxy, lower alkylthio or the like at the position 4; R3 is H, lower alkoxy, lower haloalkyl, lower cycloalkyl, (substituted) aryl, (substituted) aryloxy, (substituted) nitrogenous heterocyclic residue, (substituted) aminocarbonyl or lower alkyl--carbonyl; A is a single bond, lower alkylene or lower alkenylene; X is O or S; and the broken line between the carbon atoms at the positions 4 and 5 represents a single or double bond. These compounds exhibit excellent inhibitory activity against the production of interleukin 1.beta., thus being useful as preventive and therapeutic drugs for immunologic diseases, inflammatory diseases, ischemic diseases and so on.

ARYLPYRIDAZINONES AS PROSTAGLANDIN ENDOPEROXIDE H SYNTHASE BISOYNTHESIS INHIBITORS

The present invention describes pyridazinone compounds of formula III, which are cyclooxygenase (COX) inhibitors, and in particular, are selective inhibitors of cyclooxygenase-2 (COX/2), COX-2 us the inducible isoform associated with inflammation, as opposed to the constitutive isoform, cyclooxygenase-1 (COX- 1) which is an important "housekeeping" enzyme in many tissues, including the gastrointestinal (GI) tract and the kidneys. The selectivity of these compounds for COX-2 minimizes the unwanted GI and renal side-effects seen with current ly marked non-steroidal anti-inflammatory drugs (NSAIDs).

ЗАМЕЩЁННЫЕ ГЕТЕРОАРИЛЬНЫЕ И ФЕНИЛСУЛЬФАМОИЛЬНЫЕ СОЕДИНЕНИЯ

Настоящее изобретение относится к замещенным гетероарильным и фенилсульфамоильным соединениям, фармацевтическим композициям, содержащим такие соединения, и к применению таких соединений в качестве агонистов рецептора, активируемого пролифератором пероксисом (PPAR). Предлагаются активаторы PPAR-альфа, фармацевтические композиции, содержащие такие соединения, и применение таких соединений для повышения уровней некоторых липидов в плазме, включая холестерин липопротеидов высокой плотности, и для снижения уровней некоторых других липидов в плазме, таких как холестерин ЛНП и триглицериды, и соответственно для лечения заболеваний, которые обостряются низкими уровнями холестерина ЛВП и/или высокими уровнями холестерина ЛНП и триглицеридов, таких как атеросклероз и сердечно-сосудистые заболевания, у млекопитающих, включая человека. Соединения также применимы для лечения отрицательного баланса энергии (NEB) и связанных заболеваний у жвачных животных.

ПРОИЗВОДНЫЕ ПИРИДАЗИНОНА КАК АГОНИСТЫ РЕЦЕПТОРА ТИРЕОИДНОГО ГОРМОНА

Описаны соединения формулы (І): , (I) а также их фармацевтически приемлемые соли, где заместители являются такими, как определено в описании. Эти соединения и фармацевтические композиции, которые их содержат, являются полезными для лечения заболеваний, таких как ожирение, гиперлипидемия, гиперхолестеринемия и диабеты, и другие близкие нарушения и заболевания, и могут использоваться для лечения других заболеваний, таких как NASH, атеросклероз, сердечно-сосудистые заболевания, гипотиреоидизм, рак щитовидной железы и другие близкие нарушения и заболевания.

PYRIDAZINONE COMPOUNDS AND THEIR USE AS DAAO INHIBITORS

PIRIDAZINONOVYE HERBICIDES

Method for preparation of fungicides combination and its usage

DERIVED FROM PYRIDAZINS AND THEIR APPLICATION LIKE FUNGICIDES

Derived from sulfonyl-pyridazin

PHENYLAMIDINES HAVING A HIGH FUNGICIDAL ACTIVITY AND USE THEREOF

New phenylamidines are described, having general formula (I): 4. Fungicidal compositions comprising one or more compounds having formula (I) claim 1 , according to claim 1 , a solvent and/or a solid or liquid diluent claim 1 , optionally a surfactant.5. The compositions according to claim 4 , also comprising active principles compatible with the compounds having general formula (I) claim 4 , selected from fungicides other than the compounds having general formula (I) claim 4 , phytoregulators claim 4 , antibiotics claim 4 , herbicides claim 4 , insecticides claim 4 , fertilizers and/or mixtures thereof claim 4 , antifreeze agents claim 4 , adhesion agents.6. The compositions according to claim 4 , wherein the concentration of compounds having general formula (I) ranges from 1 to 90% by weight with respect to the total weight of the composition claim 4 , preferably from 5 to 50% by weight with respect to the total weight of the composition.8. Use of the compounds according to claim 2 , for the control of phytopatogenic fungi in agricultural crops.9. Use of the compositions according to for the control of phytopatogenic fungi in agricultural crops.10PucciniaUstilagoTilletiaUromycesPhakopsoraRhizoctoniaErysipheSphaerothecaPodosphaeraUncinulaHelminthosporiumRhynchosporiumPyrenophoraMoniliniaSclerotiniaSeptoriaMycosphaerellaVenturiaBotrytisAlternariaFusariumCercosporaCercosporella herpotrichoides, ColletotrichumPyricularia oryzae, SclerotiumPhytophtoraPythiumPlasmopara viticola, PeronosporaPseudoperonospora cubensis, Bremia lactucae.. Use according to claim 7 , for the control of phytopatogenic fungi belonging to the group of Basidiomycetes claim 7 , Ascomycetes claim 7 , Deuteromycetes or imperfect fungi claim 7 , Oomycetes: spp. claim 7 , spp. claim 7 , spp. claim 7 , spp. claim 7 , spp. claim 7 , spp. claim 7 , spp. claim 7 , spp. claim 7 , spp. claim 7 , spp. claim 7 , spp. claim 7 , spp. claim 7 , spp. claim 7 , spp. claim 7 , spp. claim 7 , spp. (spp.) claim 7 , ...

METHOD FOR PRODUCING PYRIDAZINONE COMPOUNDS AND INTERMEDIATE THEREOF

The present invention relates to a novel method for producing a pyridazinone compound and an intermediate thereof as shown in the following scheme: wherein the symbols are as defined in the specification. 2. The method according to claim 1 , wherein n is an integer of 2.3. The method according to claim 1 , wherein G is a phenyl group wherein the phenyl group may optionally have one or more substituents selected from the Group R claim 1 , provided that when it has two or more substituents claim 1 , then the substituents may be same or different.4. The method according to claim 1 , wherein the Group Ris Group R;{'sup': '4-1', 'wherein the Group Rconsists of halogen, a cyano group, a nitro group, a C1-C6 alkyl group, a C1-C6 alkoxy group, a C3-C6 cycloalkyl group, a C2-C6 alkynyl group, and a phenyl group;'}{'sup': '4-1', 'in the Group R, the C1-C6 alkyl group, the C1-C6 alkoxy group, the C3-C6 cycloalkyl group, and the C2-C6 alkynyl group may be optionally substituted with one or more halogens, provided that when they are substituted with two or more halogens, then the halogens may be same or different; and'}the phenyl group may optionally have one or more substituents selected from Group 4-1, provided that when it has two or more substituents, then the substituents may be same or different;the Group 4-1 consists of halogen and a C1-C6 alkyl group;in the Group 4-1, the C1-C6 alkyl group may be optionally substituted with one or more halogens, provided that when it is substituted with two or more halogens, then the halogens may be same or different.5. The method according to claim 4 , wherein Ris hydrogen claim 4 , a C1-C6 alkyl group or a phenyl group claim 4 ,{'sup': '2', 'Ris hydrogen, a C1-C6 alkyl group or a phenyl group wherein the C1-C6 alkyl group may be optionally substituted with one or more halogens, provided that when it is substituted with two or more halogens, then the halogens may be same or different, and the phenyl group may optionally have one or more ...

Necroptosis Inhibitors and Methods of Use Therefor

Described herein are compositions that inhibit the production of TNFα downstream of CD40 activation. As such, also described are various methods of using compositions exhibiting this activity for the treatment or prevention of inflammatory diseases associated with TNFα production or CD40 activation. 2170-. (canceled)172. A therapeutic method of treating an inflammatory disease or other disease for inhibition of CD40 mediated TNFα production claim 1 , comprising administering to a subject an effective amount of a compound of .176. The method of claim 172 , wherein the subject is a subject in need thereof; and the subject in need thereof is a subject who has been diagnosed with an inflammatory disease or a subject who is at high risk for an inflammatory disease.177. The method of claim 172 , wherein the method is a method of treating an inflammatory disease; and the inflammatory diseases is inflammatory bowel disease claim 172 , rheumatoid arthritis claim 172 , psoriatic arthritis claim 172 , psoriasis claim 172 , diabetes mellitus claim 172 , Alzheimer's disease claim 172 , refractory asthma claim 172 , multiple sclerosis claim 172 , atherosclerosis claim 172 , or vasculitis.178. The method of claim 174 , wherein the subject is a subject in need thereof; and the subject in need thereof is a subject who has been diagnosed with an inflammatory disease or a subject who is at high risk for an inflammatory disease.179. The method of claim 174 , wherein the method is a method of treating an inflammatory disease; and the inflammatory diseases is inflammatory bowel disease claim 174 , rheumatoid arthritis claim 174 , psoriatic arthritis claim 174 , psoriasis claim 174 , diabetes mellitus claim 174 , Alzheimer's disease claim 174 , refractory asthma claim 174 , multiple sclerosis claim 174 , atherosclerosis claim 174 , or vasculitis.180. The method of claim 175 , wherein the subject is a subject in need thereof; and the subject in need thereof is a subject who has been ...

PYRIDAZINONE HERBICIDES

Disclosed are compounds of Formula 1, including all stereoisomers, N-oxides, and salts thereof, 123.-. (canceled)25. The compound of wherein{'sub': 3', '3, 'X is O, S, —CH═CH—, —C(CH)═CH—, —CH═CF—, —CH═CCl— or —CH═C(CH)—;'}{'sup': '1', 'sub': 1', '7', '3', '8', '3', '8', '4', '7', '3', '7', '3', '7', '3', '7', '4', '7', '2', '3', '1', '4', '2', '7', '1', '7', '3', '7', '2', '7', '3', '7', '1', '7, 'Ris H, C-Calkyl, C-Calkylcarbonylalkyl, C-Calkoxycarbonylalkyl, C-Calkylcycloalkyl, C-Calkenyl, C-Calkynyl, C-Ccycloalkyl, C-Ccycloalkylalkyl, C-Ccyanoalkyl, C-Cnitroalkyl, C-Chaloalkoxyalkyl, C-Chaloalkyl, C-Chaloalkenyl, C-Calkoxyalkyl, C-Calkylthioalkyl, C-Calkoxy, benzyl or phenyl;'}{'sup': '2', 'sub': 1', '7', '3', '8', '3', '8', '2', '4', '2', '7', '4', '7', '3', '7', '3', '7', '1', '4', '1', '4', '1', '4', '2', '8', '3', '7', '4', '7', '2', '3', '1', '4', '2', '7', '1', '7', '3', '7', '2', '7', '1', '7', '1', '5, 'Ris H, halogen, —CN, —CHO, C-Calkyl, C-Calkylcarbonylalkyl, C-Calkoxycarbonylalkyl, C-Calkylcarbonyl, C-Calkylcarbonyloxy, C-Calkylcycloalkyl, C-Calkenyl, C-Calkynyl, C-Calkylsulfinyl, C-Calkylsulfonyl, C-Calkylamino, C-Cdialkylamino, C-Ccycloalkyl, C-Ccycloalkylalkyl, C-Ccyanoalkyl, C-Cnitroalkyl, C-Chaloalkoxyalkyl, C-Chaloalkyl, C-Chaloalkenyl, C-Calkoxyalkyl, C-Calkoxy or C-Calkylthio;'}{'sup': '3', 'sub': 1', '3', '2', '4', '2', '4', '3', '4', '1', '3', '1', '3', '1', '2', '1', '2', '1', '2, 'each Ris independently halogen, —CN, C-Calkyl, C-Calkenyl, C-Calkynyl, C-Ccycloalkyl, C-Chaloalkyl, C-Calkoxy, C-Chaloalkoxy, C-Calkylthio or C-Chaloalkylthio;'}{'sup': '4', 'sub': 1', '3', '2', '4', '2', '4', '3', '4', '1', '3', '1', '3', '1', '2', '1', '2', '1', '2, 'Ris halogen, —CN, C-Calkyl, C-Calkenyl, C-Calkynyl, C-Ccycloalkyl, C-Chaloalkyl, C-Calkoxy, C-Chaloalkoxy, C-Calkylthio or C-Chaloalkylthio; and'}n is 0, 1, 2 or 3.26. The compound of wherein{'sub': 3', '3, 'X is —CH═CH—, —C(CH)═CH—, —CH═CF—, —CH═CCl— or —CH═C(CH)—;'}{'sup': '1', 'sub': 1', '7', ' ...

PYRIDAZINONE COMPOUNDS AND THEIR USE AS DAAO INHIBITORS

The present invention provides compounds of formula (I) and pharmaceutically acceptable salts thereof, wherein Rand Rare as defined in the specification, processes for their preparation, pharmaceutical compositions containing them and their use in therapy. 2. The compound according to claim 1 , wherein Rrepresents a hydrogen atom.3. The compound according to claim 1 , wherein Y is chosen from a bond or —CRR—.5. The compound according to claim 4 , wherein each Rindependently is chosen from a hydrogen atom or methyl group.6. The compound according to claim 1 , wherein Ris chosen from phenyl claim 1 , pyridinyl claim 1 , oxazolyl claim 1 , pyrazinyl claim 1 , cyclopropyl claim 1 , cyclopentyl claim 1 , cyclohexyl claim 1 , tetrahydropyranyl claim 1 , 2 claim 1 ,3-dihydrobenzofuranyl claim 1 , pyrimidinyl claim 1 , imidazo[1 claim 1 ,2-a]pyridinyl claim 1 , pyrazolyl claim 1 , thiazolyl or piperidinyl claim 1 , and wherein the ring system is unsubstituted or substituted.7. The compound according to claim 1 , wherein Ris chosen from an unsubstituted or substituted 3- to 6-membered saturated or unsaturated carbocyclic or heterocyclic ring system.8. The compound according to claim 7 , wherein Ris chosen from a 5- or 6-membered unsaturated carbocyclic or heterocyclic ring system claim 7 , wherein the heterocyclic ring system comprises one or two ring heteroatoms independently chosen from nitrogen and oxygen claim 7 , and{'sub': 1', '4', '2', '4', '1', '2', '1', '2', '1', '4', '1', '2', '1', '4', '1', '4', '1', '4', '1', '4', '1', '4', '1', '4', '1', '4', '1', '4', '3', '6', '3', '6', '3', '6', 'p', '2', 'q, 'sup': '7', 'wherein the carbocyclic or heterocyclic ring system is unsubstituted or substituted by one, two, three or four substituents independently chosen from fluorine, chlorine, bromine, hydroxyl, cyano, oxo, C-Calkyl, C-Calkenyl, C-Chaloalkyl, C-Chydroxyalkyl, C-Calkoxy, C-Chaloalkoxy, C-Calkylthio, C-Calkylsulphinyl, C-Calkylsulphonyl, C-Calkylcarbonyl, C- ...

Ror gamma (rory) modulators

Treatment methods including administering a compound according to Formula (I) Meta or para or a pharmaceutically acceptable salt thereof wherein: A 11 -A 14 are N or CR 11 , CR 12 , CR 13 , CR 14 , respectively, with the proviso that no more than two of the four positions A in A 11 -A 14 are simultaneously N; A 6 , A 7 , A 8 , A 9 , A 10 are N or CR 6 , CR 7 , CR 8 , CR 9 , CR 10 , respectively, with the proviso that at least one but no more than two of the five positions A in A 6 , A 7 , A 8 , A 9 , A 10 is N; R 1 is C(2-6)alkyl, C(3-6)cycloalkyl, C(3-6)cycloalkylC(1-3)alkyl, (di)C(3-6)cycloalkylamino or (di)(C(3-6)cycloalkylC(1-3)alkyl)amino; R 5 is H, hydroxyethyl, methoxyethyl, C(1-6)alkyl, C(6-10)aryl, C(6-10)arylC(1-3)alkyl, C(1-9)heteroaryl, C(1-9)heteroarylC(1-3)alkyl, C(3-6)cycloalkyl, C(3-6)cycloalkylC(1-3)alkyl, C(2-5) heterocycloalkyl or C(2-5)heterocycloalkylC(1-3)alkyl; —SO 2 R 1 is represented by one of R 7 , R 8 or R 9 ; R 15 is H, C(1-6)alkyl, C(3-6)cycloalkyl, C(3-6)cycloalkylC(1-3)alkyl, C(6-10)aryl, C(6-10)arylC(1-3)alkyl, C(1-9)heteroaryl, C(1-9)heteroarylC(1-3)alkyl, C(2-5)heterocycloalkyl or C(2-5)heterocycloalkyl-C(1-3)alkyl; R 16 is C(1-6)alkyl, C(3-6)cycloalkyl, C(3-6)cycloalkylC(1-3)alkyl, C(6-10)aryl, C(6-10)arylC(1-3)alkyl, C(1-9)heteroaryl, C(1-9)heteroarylC(1-3)alkyl, C(2-5)heterocycloalkyl or C(2-5)heterocycloalkyl-C(1-3)alkyl.

METHOD FOR PRODUCING PYRIDAZINE COMPOUND

A pyridazine compound represented by formula [1]: which is useful as an active ingredient of a plant disease control agent can be produced, by steps of obtaining a compound represented by formula [3]: by reacting a compound represented by formula [4]: with a compound represented by formula [5]: obtaining a compound represented by formula [2]: by deprotecting the compound [3]; and reacting the compound [2] with a chlorinating agent. The present invention relates to a method for producing a pyridazine compound, its production intermediate, and a method for producing the same.In U.S. Pat. No. 7,569,518, a compound represented by formula [1]:wherein X represents a hydrogen atom, a fluorine atom, a chlorine atom or a methyl group, and Y represents a hydrogen atom, a fluorine atom, a chlorine atom or a methyl group, and the like are useful as an active ingredient of a plant disease control agent was described, and an advantageous production method thereof has been desired.In addition, US 2009/156608 discloses a certain type of pyridazine compounds.The present invention provides a method for producing a pyridazine compound represented by the formula [1], its production intermediate, and a method for producing the production intermediate.More specifically, the present invention is as described below.<<1>> A method for producing a compound [1] comprising steps of; obtaining a compound represented by formula [3]:wherein Q represents a protective group that is an optionally halogenated C1 to C12 alkylsulfonyl group, a C6 to C24 arylsulfonyl group optionally substituted with at least one atom or group selected from group A, or a benzyl group in which at least one hydrogen atom on the benzene ring is optionally substituted with an atom or a group selected from group B, X represents a hydrogen atom, a halogen atom or a methyl group, and Y represents a hydrogen atom, a halogen atom or a methyl group, (hereinafter described as compound [3]) Group A: a group consisting of optionally ...

2-(HETERO)ARYLPYRIDAZINONES AND THEIR USE AS HERBICIDES

2-(Hetero)arylpyradazinones of the general formula (I) are described as herbicides. 2. The 2-(hetero)arylpyridazinone or salt as claimed in in which{'sup': '1', 'sub': 1', '6', '3', '6', '2', '6', '2', '6', '1', '6', '1', '6', '1', '3', '3', '6', '1', '3', '1', '6', 'n, 'Rrepresents hydrogen, halogen, cyano, (C-C)-alkyl, (C-C)-cycloalkyl, (C-C)-alkenyl, (C-C)-alkynyl, halo-(C-C)-alkyl, (C-C)-alkoxy-(C-C)-alkyl, (C-C)-cycloalkyl-(C-C)-alkyl, amino or (C-C)-alkyl-(O)S;'}{'sup': '2', 'sub': 1', '6', '2', '6', '2', '6', '1', '6', '1', '6', 'n, 'Rrepresents hydrogen, halogen, cyano, (C-C)-alkyl, (C-C)-alkenyl, (C-C)-alkynyl, halo-(C-C)-alkyl or (C-C)-alkyl-(O)S;'}{'sup': '3', 'Rrepresents hydrogen,'}{'sup': '4', 'sub': 1', '6', '3', '6', '1', '6', '2', '6', '2', '6', '1', '6', '1', '6', '1', '3', '1', '6', '2', '6', '1', '6', '2', '6', '1', '3', '1', '6', '1', '6', '1', '3', '1', '6', '1', '6', 'n', '1', '3', '1', '3', '1', '3', '1', '3', '1', '3', 'n', '1', '3', 'n', '1', '3', '1', '3', 'n', '1', '3', 'n', '1', '3', '1', '3', '1', '3', '1', '3', '1', '3', '1', '3', '1', '3', 'n', '1', '3', '1', '3', '1', '3', '1', '3, 'Rrepresents hydroxy, halogen, cyano, nitro, (C-C)-alkyl, (C-C)-cycloalkyl, halo-(C-C)-alkyl, (C-C)-alkenyl, (C-C)-alkynyl, (C-C)-alkoxy, (C-C)-alkoxy-(C-C)-alkyl, (C-C)-alkoxy-(C-C)-alkoxy, (C-C)-alkoxy-(C-C)-alkoxy-(C-C)-alkyl, halo-(C-C)-alkoxy, halo-(C-C)-alkoxy-(C-C)-alkyl, (C-C)-alkyl-(O)S, halo-(C-C)-alkyl-(O)S, aryl, heterocyclyl, aryloxy, heterocyclyl-(C-C)-alkoxy-(C-C)-alkyl, (C-C)-alkylamino, di-(C-C)-alkylamino, (C-C)-alkylamino-(O)S, (C-C)-alkylamino-(O)S—(C-C)-alkyl, di-(C-C)-alkylamino-(O)S, di-(C-C)-alkylamino-(O)S—(C-C)-alkyl, (C-C)-alkylamino-(O)C, di-(C-C)-alkylamino-(O)C, di-(C-C)-alkylamino-(O)C—(C-C)-alkyl, (C-C)-alkyl-(O)C-amino or (C-C)-alkyl-(O)S-amino, where the heterocyclyl groups and aryl groups are substituted by s radicals from the group consisting of (C-C)-alkyl, halo-(C-C)-alkyl, (C-C)-alkoxy, halo-(C-C)-alkoxy, cyano, nitro ...

Pyridazinone compounds and their use as daao inhibitors

The present invention provides compounds of formula (I) and pharmaceutically acceptable salts thereof, wherein R 1 and R 2 are as defined in the specification, processes for their preparation, pharmaceutical compositions containing them and their use in therapy.

ROR GAMMA (RORY) MODULATORS

Novel compounds according to Formula I 2. The compound according to wherein:{'sub': 11', '14', '11', '12', '13', '14', '1', '14, 'A-Aare N or CR, CR, CR, CR, respectively, with the proviso that no more than two of the four positions A in A-Acan be simultaneously N;'}{'sub': 6', '7', '9', '10', '6', '7', '9', '10', '6', '7', '9', '10, 'A, A, A, Aare N or CR, CR, CR, CR, respectively, with the proviso that at least one but no more than two of the four positions A in A, A, A, Ais N;'}{'sub': 8', '8, 'Ais CR;'}{'sub': '1', 'Ris C(3-6)cycloalkylC(1-3)alkyl or (di)C(3-6)cycloalkylamino with all carbon atoms of alkyl groups optionally substituted with one or more F and all carbon atoms of cycloalkyl groups optionally substituted with one or more F or methyl;'}{'sub': 2', '3, 'Rand Rare independently H;'}{'sub': '4', 'Ris H;'}{'sub': '5', 'Ris H, hydroxyethyl, methoxyethyl, C(1-6)alkyl, C(2-5)heterocycloalkyl or C(2-5)heterocycloalkylC(1-3)alkyl, all groups optionally substituted with one or more F, C(1-2)alkoxy or cyano;'}{'sub': 1', '8, 'the sulfonyl group with Ris represented by R;'}{'sub': 6', '14, 'the remaining R-Rare independently H, halogen, C(1-3)alkoxy or C(1-6)alkyl, all of the alkyl groups optionally being substituted with one or more F or hydroxy; and'}{'sub': '15', 'Ris C(1-6)alkyl or C(3-6)cycloalkyl, all groups optionally substituted with one or more F, C(1-2)alkoxy or cyano;'}{'sub': '16', 'and Ris C(1-6)alkyl, C(3-6)cycloalkyl, C(3-6)cycloalkylC(1-3)alkyl, C(6-10)aryl, C(2-5)heterocycloalkyl or C(2-5)heterocycloalkyl-C(1-3)alkyl, all groups optionally substituted with one or more F, C(1-2)alkyl, C(1-2)alkoxy or cyano.'}3. The compound according to wherein:{'sub': 11', '14', '11', '12', '13', '14, 'A-Aare respectively CR, CR, CR, CR;'}{'sub': 6', '7', '9', '10', '6', '7', '9', '10', '6', '7', '9', '10, 'A, A, A, Aare N or CR, CR, CR, CR, respectively, with the proviso that at least one but no more than two of the four positions A in A, A, A, Ais N;'}{'sub': ...

Cyclohexanone compounds and herbicides comprising the same

The present invention provides a compound having an excellent efficacy for controlling weeds. A cyclohexanone compound of the formula (I): wherein m is an integer of 1, 2 or 3; n is an integer of any one of 1 to 5; X represents CH 2 , O, S, S(O) or S(O) 2 ; R 1 represents a hydrogen atom or a methyl group; R 2 and R 3 represents a hydrogen atom, a C 1-6 alkyl group and the like; R 4 represents a C 6-10 aryl group or a five- to six-membered heteroaryl group; G represents a hydrogen atom and the like; Z represents a halogen atom, a cyano group, a nitro group, a phenyl group, a C 1-6 alkyl group and the like; is useful as an active ingredient for herbicides.

Pyridazine derivatives as EAAT2 Activators

Pyridazine derivatives that activate the excitatory amino acid transporter 2 (EAAT2), and methods of use thereof for treating or preventing diseases, disorders, and conditions associated with glutamate excitotoxicity. 2. The method of claim 1 , wherein Ris 2-pyridyl.3. The method of claim 1 , wherein X is S claim 1 , S(O) claim 1 , SO; O claim 1 , NH claim 1 , N(C-Calkyl) claim 1 , or a bond.4. (canceled)5. The method of claim 1 , wherein X is CH.6. The method according to claim 1 , wherein Ris —Y—R.7. The method of claim 6 , wherein Y is C-Calkylene.8. The method of claim 1 , wherein Ris independently selected from: (a) C-Caryl claim 1 , which is optionally substituted with from 1-5 independently selected R claim 1 , and (b) heteroaryl claim 1 , which contains from 5-10 ring atoms claim 1 , wherein from 1-4 of the ring atoms is independently selected from N claim 1 , NH claim 1 , N(C-Calkyl) claim 1 , O claim 1 , and S; and wherein said heteroaryl ring is optionally substituted with from 1-5 independently selected R.9. The method of claim 6 , wherein Ris C-Caryl claim 6 , which is optionally substituted with from 1-5 independently selected R.10. The method of claim 9 , wherein Ris C-Calkyl or halo.11. (canceled)13. (canceled)14. The method of claim 12 , wherein one of Rand Ris R claim 12 , and the other of Rand Ris an independently selected Rand/or Ris an independently selected R.15. The method according to claim 12 , wherein each occurrence of Ris an independently selected C-Calkyl claim 12 , a fluoro claim 12 , or a chloro.16. (canceled)17. The method according to claim 9 , wherein{'sup': '5', 'Ris2-methylphenyl,2-chlorophenyl,2,6-dimethylphenyl,2,4-dimethylphenyl,2,6-dichlorophenyl,2-fluorophenyl,2,4-difluorophenyl,3-chlorophenyl,2,4,6-trimethylphenyl,2-chloro-6-fluorophenyl,2,3-dichlorophenyl,2,4-dichlorophenyl,2,5-dichlorophenyl,2,6-difluorophenyl,2,4,6-trifluorophenyl,4-fluorophenyl,2-chloro-4-fluorophenyl,3-methylphenyl,2-azido-4-(hex-5-yn-1-yloxy)phenyl,6- ...

FLUORINATED BENZENESULFONAMIDES AS INHIBITORS OF CARBONIC ANHYDRASE

Novel fluorinated benzenesulfonamides compounds of general formula (I) 15-. (canceled)7. Fluorinated benzenesulfonamides according to claim 6 , selected from a group comprising of:2,3,5,6-tetrafluoro-4-hydrazinobenzenesulfonamide;4-(2-benzylidenehydrazino)-2,3,5,6-tetrafluorobenzenesulfonamide;2,3,5,6-tetrafluoro-4[(2-hydroxyethyl)thio]benzenesulfonamide;2,3,5,6-tetrafluoro-4[(2-hydroxyethyl)sulfonyl]benzenesulfonamide;2-{[4-(aminosulfonyl)-2,3,5,6-tetrafluorophenyl]sulfonyl}ethyl acetate;2,3,5,6-tetrafluoro-4-(propylthio)benzenesulfonamide;{[4-(aminosulfonyl)-2,3,5,6-tetrafluorophenyl]thio}acetic acid;3-{[4-(aminosulfonyl)-2,3,5,6-tetrafluorophenyl]thio}propanoic acid;6-{[4-(aminosulfonyl)-2,3,5,6-tetrafluorophenyl]amino}hexanoic acid;2,3,5,6-tetrafluoro-4-(phenylthio)benzenesulfonamide;2,3,5,6-tetrafluoro-4-(phenylsulfonyl)benzenesulfonamide;2,3,5,6-tetrafluoro-4-phenoxybenzenesulfonamide;4-(benzylthio)-2,3,5,6-tetrafluorobenzenesulfonamide;4-(benzylamino)-2,3,5,6-tetrafluorobenzenesulfonamide;2,3,5,6-tetrafluoro-4-{[2-(4-hydroxyphenyl)ethyl]amino}benzenesulfonamide;2,3,5,6-tetrafluoro-4-[(2-phenylethyl)thio]benzenesulfonamide;2,3,5,6-tetrafluoro-4-[(2-phenylethyl)sulfonyl]benzenesulfonamide;2,3,5,6-tetrafluoro-4-morpholin-4-ylbenzenesulfonamide;2,3,5,6-tetrafluoro-4-[(mesitylmethyl)thio]benzenesulfonamide;4-[(4,6-dimethylpyrimidin-2-yl)thio]-2,3,5,6-tetrafluorobenzenesulfonamide;4-(1,3-benzothiazol-2-ylthio)-2,3,5,6-tetrafluorobenzenesulfonamide;4-(1-adamantylamino)-2,3,5,6-tetrafluorobenzenesulfonamide;3-{[4-(aminosulfonyl)-2,3,5,6-tetrafluorophenyl]thio}-[1,2,3]thiadiazolo[3,4-a]benzimidazole;4-[(4,5-diphenyl-1H-imidazol-2-yl)thio]-2,3,5,6-tetrafluorobenzenesulfonamide;2-(isopropylamino)-3,5,6-trifluoro-4-[(2-phenylethyl)thio]benzenesulfonamide;2-(benzylamino)-3,5,6-trifluoro-4-[(2-phenylethyl)thio]benzenesulfonamide;2-[(2-phenylethyl)amino]-3,5,6-trifluoro-4-[(2-phenylethyl)thio]benzenesulfonamide;2-[(1-phenylethyl)amino]-3,5,6-trifluoro-4-[(2-phenylethyl)thio ...

SULFONYLUREAS AND SULFONYLTHIOUREAS AS NLRP3 INHIBITORS

The present invention relates to compounds of formula (I): 2. The compound or a pharmaceutically acceptable salt claim 1 , solvate or prodrug thereof claim 1 , as claimed in claim 1 , wherein Ris a 6-membered heteroaryl group containing at least two nitrogen atoms in the 6-membered ring structure claim 1 , wherein Rmay optionally be substituted claim 1 , and wherein optionally:(i) at least one of the two nitrogen atoms is located at the 3, 4 or 5-position of the 6-membered ring structure; or(ii) a first nitrogen atom is located at the 2-position and a second nitrogen atom is located at the 6-position of the 6-membered ring structure, and wherein the 6-membered heteroaryl group is substituted with one or more monovalent groups at the 3- and/or 5-positions of the 6-membered ring structure.34-. (canceled)5. The compound or a pharmaceutically acceptable salt claim 1 , solvate or prodrug thereof claim 1 , as claimed in claim 1 , wherein the 6-membered heteroaryl group of Ris substituted with at least one monovalent group X claim 1 , wherein X is at each occurrence any group that can mesomerically donate a lone pair of electrons from a nitrogen claim 1 , oxygen or sulphur atom onto at least one nitrogen atom in the 6-membered ring structure claim 1 , and wherein the 6-membered heteroaryl group may optionally be further substituted.6. The compound or a pharmaceutically acceptable salt claim 1 , solvate or prodrug thereof claim 1 , as claimed in claim 1 , wherein:{'sup': '1', 'the 6-membered heteroaryl group of Ris substituted with at least one monovalent group X′ at a position ortho- or para- to at least one nitrogen atom in the 6-membered ring structure;'}{'sup': '1', 'the 6-membered heteroaryl group of Rmay optionally be further substituted;'}{'sup': '1', 'Xis at each occurrence independently selected from a'}{'sup': 3', '3', '3', '3', '3', '3', '3', '3', '3', '3', '3', '3', '3', '3', '3, 'sub': 2', '2', '2', '2, '—OR, —SR, —N(R), —O-L-OR, —O-L-SR, —O-L-N(R), —S-L-OR, —S ...

Novel pyridazine derivatives and drugs containing the same as the active ingredient

This invention relates to pyridazine derivatives represented by the formula (1): wherein R 1 represents a (substituted) aryl group, R 2 represents a phenyl group substituted at 4-position by a lower alkoxyl group or a lower alkylthio group, R 3 represents a lower alkoxyl group, a halogenated lower alkyl group, a lower cycloalkyl group, a (subsituted) aryl group, a (substituted) aryloxy group, a (substituted) nitrogen-containing heterocyclic ring residue, a (substituted) aminocarbonyl group or a lower alkylcarbonyl group, A represents a single bond, a lower alkylene group or a lower alkenylene group, X represents O or S, and the dashed line indicates that the carbon-carbon bond between the 4-position and the 5-position is a single bond or a double bond, or salts thereof; and also to medicines containing them as effective ingredients. These compounds have excellent inhibitory activity against interleukin-1β production, and are useful as preventives and therapeutics for immune system diseases, inflammatory diseases, ischemic diseases and the like.

新颖的哒嗪衍生物和含有其作为有效成分的药物

本发明涉及由式(1)代表的哒嗪衍生物或其盐:其中R 1 代表(取代的)芳基,R 2 代表苯基,在4－位被低级烷氧基或低级烷硫基取代,R 3 代表低级烷氧基、卤代低级烷基、低级环烷基、(取代的)芳基、(取代的)芳氧基、(取代的)含氮杂环残基、(取代的)氨基羰基、或低级烷基羰基,A代表单键、低级亚烷基或低级亚烯基,X代表O或S,虚线表示4－位与5－位之间的碳－碳键是单键或双键;本发明也涉及含有其作为有效成分的药物。这些化合物具有极佳的抗白介素－1β生成的抑制活性,可用作免疫系统疾病、炎性疾病、局部缺血性疾病等的预防剂和治疗剂。

Производные пиридазинона в качестве агонистов рецептора тиреоидного гормона

Изобретение относится к соединениям общей формулы (I), где: А представляет собой О, СН2, S, SO или SO2; Х и Y выбраны из Br, Cl и -СН3; R1 выбран из группы, состоящей из -(CH2)nCOOH, -NHC(=O)COOH, -NHCH2COOH, ! ! Z представляет собой Н или -C≡N; R2 - низший алкил; R3 - Н или низший алкил; n означает 1, 2 или 3; р означает 1 или 2; или к их фармацевтически приемлемым солям или сложным эфирам. Кроме того, изобретение относится к фармацевтической композиции на основе указанных соединений, обладающей агонистической активностью в отношении рецептора тиреоидного гормона. Указанные соединения и содержащие их фармацевтические композиции могут быть полезными для лечения таких заболеваний, как ожирение, гиперлипидемия, гиперхолестеринемия и диабеты, и других близких нарушений и заболеваний, и могут использоваться для лечения других заболеваний, таких как NASH, атеросклероз, сердечно-сосудистые заболевания, гипотироидизм, рак щитовидной железы и других близких нарушений и заболеваний. 2 н. и 23 з.п. ф-лы, 1 табл. РОССИЙСКАЯ ФЕДЕРАЦИЯ (19) RU (11) 2 379 295 (13) C2 (51) МПК C07D 237/14 (2006.01) A61K 31/495 (2006.01) A61P 5/14 (2006.01) ФЕДЕРАЛЬНАЯ СЛУЖБА ПО ИНТЕЛЛЕКТУАЛЬНОЙ СОБСТВЕННОСТИ, ПАТЕНТАМ И ТОВАРНЫМ ЗНАКАМ (12) ОПИСАНИЕ ИЗОБРЕТЕНИЯ К ПАТЕНТУ (24) Дата начала отсчета срока действия патента: 11.07.2006 (30) Конвенционный приоритет: 21.07.2005 US 60/701,215 (43) Дата публикации заявки: 27.08.2009 (56) Список документов, цитированных в отчете о поиске: WO 99/00353 A1, 07.01.1999. EP 0188351 A2, 23.07.1986. US 5,284,971 А, 08.02.1994. WO 2004/085406 A1, 07.10.2004. RU 2209813 C2, 10.08.2003. (73) Патентообладатель(и): Ф.ХОФФМАНН-ЛЯ РОШ АГ (CH) 2 3 7 9 2 9 5 R U (86) Заявка PCT: EP 2006/064093 (11.07.2006) C 2 C 2 (85) Дата перевода заявки PCT на национальную фазу: 21.02.2008 (87) Публикация PCT: WO 2007/009913 (25.01.2007) Адрес для переписки: 101000, Москва, М.Златоустинский пер., 10, кв.15, ЕВРОМАРКПАТ, пат.пов. И.А.Веселицкой, рег. № 11 (54) ПРОИЗВОДНЫЕ ПИРИДАЗИНОНА В ...

Phenylpyridazine compounds and medicinal agents comprising thereof

FIELD: organic chemistry, medicine, pharmacy. SUBSTANCE: invention proposes phenylpyridazine compounds represented by the following formula (I): wherein R 1 represents unsubstituted or substituted phenyl wherein substitutes are taken among the group comprising halogen atom, lower alkyl, lower alkoxy-group and phenylthio-group, or pyridyl; R 2 represents lower alkoxy-group, lower alkylthio-group, lower alkylsulfinyl or lower alkylsolfonyl; R 3 represents hydrogen atom or lower alkoxy-group; or R 2 and R 3 can be condensed in common forming lower alkylenedioxy-group; R 4 represents cyano-group, carboxyl, unsubstituted or substituted lower alkyl wherein substitutes are taken among the group comprising hydroxyl, carboxyl and N-hydroxy-N-lower alkylaminocarbonyl; lower alkenyl; lower alkylthio-group; lower alkylsulfinyl; lower alkylsulfonyl; lower alkylsulfonyloxy; unsubstituted or substituted phenoxy-group wherein substitutes are taken among the group comprising halogen atom, lower alkoxy-, nitro-, cyano-group; unsubstituted phenylthio-group or phenylthio-group substituted with halogen atom; pyridyloxy-; morpholino-group; morpholinylcarbonyl; 1-piperazinylcarbonyl substituted with lower alkyl; unsubstituted or substituted amino-group wherein substitutes are taken among the group comprising lower alkyl, benzyl, phenyl that can be substituted with halogen atoms or lower alkoxy-groups, and n = 0, or their salts. Proposed compounds possess the excellent inhibitory activity against biosynthesis of interleukin-1β and can be used in preparing a medicinal agent inhibiting biosynthesis of interleukin-1β, in particular, in treatment and prophylaxis of such diseases as diseases of immune system, inflammatory diseases and ischemic diseases. Also, invention proposes intermediate compounds for preparing compounds of the formula (I). Except for, invention proposes a medicinal agent and pharmaceutical composition that inhibit biosynthesis of interleukin-1β and inhibitor of biosynthesis ...

Phenylpyridazine derivatives and drugs containing the same

본 발명은 일반식(I) The present invention is of general formula (I) (식중, R 1 은 치환기를 가져도 좋은 페닐기, 피리딜기 등을 나타내고, R 2 는 저급알콕시기, 저급알킬티오기, 저급알킬술피닐, 저급 알킬술포닐기 등을 나타내고, R 3 는 수소원자, 저급알콕시기 등을 나타내고, R 4 는 수소원자, 치환알킬기 등을 나타낸다)로 표시되는 페닐피리다진 유도체 또는 그의 염 및 이를 함유하는 의약에 관한다. (Wherein, R 1 represents a phenyl group, a pyridyl group, etc. which may have a substituent, R 2 represents a lower alkoxy group, a lower alkylthio group, a lower alkylsulfinyl, a lower alkylsulfonyl group, etc., R 3 represents a hydrogen atom, A lower alkoxy group and the like, R 4 represents a hydrogen atom, a substituted alkyl group, or the like), and a phenylpyridazine derivative or salt thereof and a medicine containing the same. 이 화합물은 우수한 인터로이킨-1β 산생 억제작용을 가기며, 면역계 질환, 염증성 질환, 허혈성 질환 등의 예방·치료제 등의 의약으로서 유용하다. This compound has an excellent interleukin-1β production inhibitory effect and is useful as a medicament for preventing and treating immune system diseases, inflammatory diseases, ischemic diseases and the like.

The preparation method of pyridazinone derivative and desinsection thereof, kill mite, nematicide, fungicide composition

本发明提供了一种3(2H)-哒嗪酮衍生物(1)式中，R 1 表示烷基，A 1 表示卤素，R 10 和R 11 表示氢原子或者低级烷基；X′表示氧原子或硫原子，Y″表示低级烷基，环烷基；低级烷氧基，低级卤代烷基，低级卤代烷氧基，或者取代苯基。本发明还提供了一种制备所说的衍生物的方法。

ROR GAMMA MODULATORS (RORγ)

РОССИЙСКАЯ ФЕДЕРАЦИЯ (19) RU (11) (13) 2017 145 928 A (51) МПК C07D 213/71 (2006.01) ФЕДЕРАЛЬНАЯ СЛУЖБА ПО ИНТЕЛЛЕКТУАЛЬНОЙ СОБСТВЕННОСТИ (12) ЗАЯВКА НА ИЗОБРЕТЕНИЕ (21)(22) Заявка: 2017145928, 03.06.2016 (71) Заявитель(и): ЛИД ФАРМА ХОЛДИНГ Б.В. (NL), САНОФИ (FR) Приоритет(ы): (30) Конвенционный приоритет: 05.06.2015 EP 15170768.4 (85) Дата начала рассмотрения заявки PCT на национальной фазе: 09.01.2018 (86) Заявка PCT: (87) Публикация заявки PCT: WO 2016/193468 (08.12.2016) A Адрес для переписки: 129090, Москва, ул. Б. Спасская, 25, стр. 3, ООО "Юридическая фирма Городисский и Партнеры" (57) Формула изобретения 1. Соединение формулы I A (Формула I) R U 2 0 1 7 1 4 5 9 2 8 (54) МОДУЛЯТОРЫ ROR ГАММА (RORγ) 2 0 1 7 1 4 5 9 2 8 EP 2016/062708 (03.06.2016) R U (43) Дата публикации заявки: 10.07.2019 Бюл. № 19 (72) Автор(ы): КАЛС, Йосеф Мария Герардус Барбара (NL), МАШНИК, Давид (FR), НАБЮЮРС, Сандер Бернардус (NL), САБЮКО, Жан-Франсуа (FR), ШИО, Лоран (FR) Стр.: 1 A 2 0 1 7 1 4 5 9 2 8 A R U 2 0 1 7 1 4 5 9 2 8 Стр.: 2 R U Мета или пара или его фармацевтически приемлемая соль, где: - A11-A14 являются N или CR11, CR12, CR13, CR14, соответственно, при условии, что не более двух из четырех положений A в A11-A14 одновременно могут быть N; - A6, A7, A8, A9,A10 являются N or CR6, CR7, CR8, CR9, CR10, соответственно, при условии, что, по крайней мере, одно, но не более двух из пяти положений A в A6, A7, A8, A9, A10 является N; - R1 является C(2-6)алкилом, C(3-6)циклоалкилом, C(3-6)циклоалкилC(1-3)алкилом, (ди)C(3-6)циклоалкиламино или (ди)(C(3-6)циклоалкилC(1-3)алкил)амино, где все атомы углерода алкильных групп необязательно замещены одним или более F и где все атомы углерода циклоалкильных групп необязательно замещены одним или более F или метилом; - R2 и R3 независимо являются H, F, метилом, этилом, гидрокси, метокси, или R2 и R3 вместе являются карбонилом, все алкильные группы, если присутствуют, необязательно замещены одним или более F; - R4 является H или C(1-6)алкилом ...

Pyridazinone herbicides

화학식 1의 화합물 (모든 입체 이성질체 포함), 이의 N -옥사이드 및 이의 염이 개시되어 있다: 상기 식에서, X는 O, S 또는 NR 5 이거나; X는 -C(R 6 )=C(R 7 )-이며, 여기서 R 6 에 결합된 탄소 원자는 R 4 에 결합된 탄소 원자에도 결합되고, R 7 에 결합된 탄소 원자는 화학식 1의 페닐환 부분에도 결합되며; R 1 , R 2 , R 3 , R 4 , R 5 , R 6 , R 7 , G 및 W는 본 명세서 및 청구범위에 정의한 바와 같다. 화학식 1의 화합물을 함유하는 조성물, 및 원하지 않는 초목 (vegetation) 또는 이의 환경을 본 발명의 화합물 또는 조성물의 유효량과 접촉시키는 단계를 포함하는, 원하지 않는 초목을 방제하는 방법도 개시되어 있다.

The preparation method of pyridazinone derivative, and insecticidal constituent kill acaricidal composition, and the nematicide composition kills (very) bacterium composition

具有通式(I)的新的3(2H)-哒嗪酮衍生物的制备方法，

Novel allylthiopyridazine derivative and process for preparing the same

PURPOSE: Provided are allylthio pyridazine derivatives represented by the chemical structure 1, pharmaceutically acceptable salts, and a preparation method thereof which show excellent medial effect against liver disease and radiation exposure. CONSTITUTION: The allylthio pyridazine derivatives and its pharmaceutically acceptable salts represented by the chemical formula I where R1 represents phenoxy, benzyloxy or phenyl substituted with halogen atom, low alkoxy, dialkyl alkoxy, hydroxyalkoxy, or low alkyl; R2, R3 respectively represent hydrogen, low alkyl or saturated/unsaturated ring containing carbon atoms therein. In case R1 is chloro, both R2 and R3 are not hydrogen. According to the present invention, the derivatives are obtained by the process of mixing allyl mercaptan with the sodium metal in anhydrous methanol; adding 3,6-dichloro-4,5-dimethyl pyridazine to the solution and refluxing; eliminating methanol and adding ether and washing the ether layer with water.

Acaricidal composition

Novel pyridazinone derivatives of the general formula (I): …<CHEM>… wherein R represents a straight or branched chain alkyl group having 2 to 6 carbon atoms, A represents halogen atom, alkoxy group having 1 to 4 carbon atoms or alkylthio group having 1 to 4 carbon atoms, X represents oxygen atom or sulfur atom,… B represents …<CHEM>… Y represents oxygen atom, sulfur atom, …<CHEM>… V represents oxygen atom or sulfur atom,… R<1> and R<2> represent independently hydrogen atom or alkyl having 1 to 4 carbon atoms,… R<3> and R<6> represent independently hydrogen atom, halogen atom, alkyl having 1 to 4 carbon atoms, cyano group, haloalkyl group having 1 to 4 carbon atom or alkoxycarbonyl group having 1 to 4 carbon atoms, R<7> represents alkyl group having 1 to 4 carbon atoms or alkylcarbonyl group having 1 to 4 carbon atoms and Z represents various specific organic groups. A process for preparation of said derivatives is also provided. These derivatives are useful as an active ingredient of insecticidal, acaricidal, nematicidal and/or fungicidal compositions for agricultural and horticultural uses as well as of expellent compositions for ticks parasitic on animals.

Herbicide agent and a method for struggle against weeds

FIELD: agriculture. SUBSTANCE: herbicide agent has 0.5-90% compound of the formula (I) where R 1 - halogen, hydroxyl, amino-, nitro-, cyano-, lower alkyl, C 5 -C 7 -cycloalkyl, trifluoromethyl, C 1 -C 6 -alkoxy, C 1 -C 4 -alkylthio, phenoxy, C 1 -C 4 -alkylsulfonyl; R 2 - hydrogen, halogen, nitro, C 1 -C 4 -alkyl, C 1 -C 4 -alkoxy; n = 1, 2; m = 0, 1; R 3 - hydroxyl, halogen, CO(O)ZR 4 , OCOCO)N(R 5 ) 2 ; R 4 -C 1 -C 12 -alkyl, C 5 -C 7 -cycloalkyl, phenyl, lower alkyl substituted with phenyl; R 5 -C 1 -C 4 -alkyl; Z - simple bond, oxygen or sulfur; X - halogen. Composition is used for struggle against weeds at the dose of active substance consumption 0.2-1.688 kg/ha. Structure of compound of the formula (I) is given in invention description. EFFECT: improved method of synthesis, increased effectiveness of herbicide. 4 cl, 14 tbl ЕЗУЗОсС ПЧ Го РОССИЙСКОЕ АГЕНТСТВО ПО ПАТЕНТАМ И ТОВАРНЫМ ЗНАКАМ (19) (51) МПК ВИ” 2 054 871 ' 13) Сл А 01 М 43/58 12) ОПИСАНИЕ ИЗОБРЕТЕНИЯ К ПАТЕНТУ РОССИЙСКОЙ ФЕДЕРАЦИИ (21), (22) Заявка: 4894984/04, 04.04.1991 (30) Приоритет: 05.04.1990 АТ А 807/90 (46) Дата публикации: 27.02.1996 (56) Ссылки: Выложенная заявка Японии 81-113767, кл. С 070237/14, опублик. 1981.Справочник по пестицидам. - М.: Химия, 1385, с.88. (71) Заявитель: Агролинц Агрархемикалиен ГмбХ (АТ) (72) Изобретатель: Дитмар Корес[АТ], Херманн Трамбергер[АТ], Рудольф Хельмут Вертер[АТ], Рудольф Иеллингер[АТ], Энгельберг Клоимштайн[АТ], Руперт Шенбек[АТ] (73) Патентообладатель: Агролинц Агрархемикалиен ГмбХ (АТ) (54) ГЕРБИЦИДНОЕ СРЕДСТВО И СПОСОБ БОРЬБЫ С СОРНЯКАМИ (57) Реферат: Использование. сельское хозяйство, химические средства защиты растений. Сущность изобретения: гербицидное средство содержит 0,5 - 90% соединения ф-лы 1, где К 1-галоген, гидроксил, амино-, нитро-, циано-, низший алкил, С - С7-циклоалкил, трифторметил, С. - Св-апкокси, С. - С д-алкилтио, фенокси, С: - С д-алкилсульфонил, К>-водород, галоген, нитро, С1 - С4-алкил, С1 - Сд-алкокси, п-1,2, т-0,1, Вз- ...

Pyrimidopyridazine derivatives applicable as p38 map kinase

FIELD: medicine, pharmaceutics. SUBSTANCE: invention refers to a compound of formula (IA) or (IB), or a pharmacologically acceptable salts thereof, wherein R 2a , R 2b , R 2c are independently specified in H, halogen and C 1 -C 6 alkyl; Y represents -O- or -S(O) p -, wherein p is equal to 0, 1 or 2; and R 1 represents a radical of formula (IIC), wherein T represents -N or -CH; R 3 represents H or F. EFFECT: invention refers to a pharmaceutical composition possessing activity inhibiting p38 MAP kinase, and using them for treating bronchopulmonary diseases. 15 cl, 4 tbl, 2 ex РОССИЙСКАЯ ФЕДЕРАЦИЯ (19) RU (11) (13) 2 516 466 C2 (51) МПК C07D 237/18 (2006.01) C07D 487/04 (2006.01) A61K 31/50 (2006.01) A61K 31/519 (2006.01) A61K 31/5377 (2006.01) A61P 11/00 (2006.01) ФЕДЕРАЛЬНАЯ СЛУЖБА ПО ИНТЕЛЛЕКТУАЛЬНОЙ СОБСТВЕННОСТИ (12) ОПИСАНИЕ (21)(22) Заявка: ИЗОБРЕТЕНИЯ К ПАТЕНТУ 2011134382/04, 16.02.2010 (24) Дата начала отсчета срока действия патента: 16.02.2010 (72) Автор(ы): БЕСВИК Аманда (GB), ВАШКОВЫЧ Богдан (GB) (73) Патентообладатель(и): КЬЕЗИ ФАРМАЧЕУТИЧИ С.П.А. (IT) Приоритет(ы): (30) Конвенционный приоритет: (43) Дата публикации заявки: 27.03.2013 Бюл. № 9 R U 17.02.2009 GB 0902648.5 (45) Опубликовано: 20.05.2014 Бюл. № 14 A1, 30.03.2000; . RU 2284187 C2, 27.09.2006 (85) Дата начала рассмотрения заявки PCT на национальной фазе: 19.09.2011 (86) Заявка PCT: GB 2010/050256 (16.02.2010) 2 5 1 6 4 6 6 (56) Список документов, цитированных в отчете о поиске: EA 2855 B1, 31.10.2002. WO 00/17204 2 5 1 6 4 6 6 WO 2010/094955 (26.08.2010) Адрес для переписки: 129090, Москва, ул. Большая Спасская, 25, стр. 3, ООО "Юридическая фирма "Городисский и Партнеры" (54) ПИРИМИДОПИРИДАЗИНОВЫЕ ПРОИЗВОДНЫЕ, ПРИГОДНЫЕ В КАЧЕСТВЕ Р38 МАРК (57) Реферат: Изобретение относится к соединению формулы (IA) или (IB), или его фармацевтически приемлемой соли, где R2a, R2b, R2c независимо выбирают из H, галогена и C1-C6алкила; Y R U представляет собой -O- или -S(O)p-, где p равно 0, 1 или 2; и R1 ...

Pyridazinone derivatives and pharmaceutical compositions comprising the same

본 발명은 화학식 Ⅰ의 피리다지논 유도체 또는 의약적으로 허용되는 이의 염 및 이를 활성 성분으로서 함유하는 의약 조성물에 관한 것이다. The present invention relates to a pyridazinone derivative of formula (I) or a pharmaceutically acceptable salt thereof and a pharmaceutical composition containing the same as an active ingredient. 화학식 Ⅰ Formula I 위의 화학식 Ⅰ에서 In Formula I above R 1 은 임의로 치환된 페닐기 또는 방향족 복소환기이며, R 1 is an optionally substituted phenyl group or aromatic heterocyclic group, R 2 는 임의로 치환된 알킬기, 페닐기, 아르알킬기, 방향족 복소환기, 아미노기, 환상 아미노기, 시아노기, 카복실기 등이며, R 2 is an optionally substituted alkyl group, phenyl group, aralkyl group, aromatic heterocyclic group, amino group, cyclic amino group, cyano group, carboxyl group and the like, R 3 은 수소원자, 임의로 치환된 알킬기, 페닐기, 방향족 복소환기이며, R 3 is a hydrogen atom, an optionally substituted alkyl group, a phenyl group, an aromatic heterocyclic group, R 4 는 시아노기, 카보닐기 등이다. R 4 is a cyano group, a carbonyl group, or the like. 피리다지논 유도체, 세포 접착 억제제, 염증, 천식, 류마티스 Pyridazinone derivatives, cell adhesion inhibitors, inflammation, asthma, rheumatism

Pyridazinone compound and herbicide and noxious arthropod controlling agent comprising it

The present invention relates to a pyridazinone compound of the formula (I): wherein R 1 represents hydrogen, a C 1-6 alkyl group, and the like, R 2 represents halogen, a cyano group, a nitro group, a C 1-6 alkoxy group, and the like, G represents hydrogen, and the like, Z represents halogen, a cyano group, a nitro group, a C 1-6 alkyl group, and the like, and n represents an integer of 1-5 useful as an active ingredient in a herbicideand a noxious arthropod controlling agent.

Patent RU2017145928A3

ВУ” 2017145928” АЗ Дата публикации: 15.10.2019 Форма № 18 ИЗ,ПМ-2011 Федеральная служба по интеллектуальной собственности Федеральное государственное бюджетное учреждение ж 5 «Федеральный институт промышленной собственности» (ФИПС) ОТЧЕТ О ПОИСКЕ 1. . ИДЕНТИФИКАЦИЯ ЗАЯВКИ Регистрационный номер Дата подачи 2017145928/04(078579) 03.06.2016 РСТ/ЕР2016/062708 03.06.2016 Приоритет установлен по дате: [ ] подачи заявки [ ] поступления дополнительных материалов от к ранее поданной заявке № [ ] приоритета по первоначальной заявке № из которой данная заявка выделена [ ] подачи первоначальной заявки № из которой данная заявка выделена [ ] подачи ранее поданной заявки № [Х] подачи первой(ых) заявки(ок) в государстве-участнике Парижской конвенции (31) Номер первой(ых) заявки(ок) (32) Дата подачи первой(ых) заявки(ок) (33) Код страны 1. 15170768.4 05.06.2015 ЕР* Название изобретения (полезной модели): [Х] - как заявлено; [ ] - уточненное (см. Примечания) МОДУЛЯТОРЫ ВОВ ГАММА (ВОВУ) Заявитель: ЛИД ФАРМА ХОЛДИНГ Б.В., МГ, САНОФИ, ЕК 2. ЕДИНСТВО ИЗОБРЕТЕНИЯ [Х] соблюдено [ ] не соблюдено. Пояснения: см. Примечания 3. ФОРМУЛА ИЗОБРЕТЕНИЯ: [Х] приняты во внимание все пункты (см. п см. Примечания [ ] приняты во внимание следующие пункты: [ ] принята во внимание измененная формула изобретения (см. Примечания) 4. КЛАССИФИКАЦИЯ ОБЪЕКТА ИЗОБРЕТЕНИЯ (ПОЛЕЗНОЙ МОДЕЛИ) (Указываются индексы МПК и индикатор текущей версии) (070 213/71 (2006.01) 5. ОБЛАСТЬ ПОИСКА 5.1 Проверенный минимум документации РСТ (указывается индексами МПК) С07О 213/71, Аб1К 31/44, Аб1Р 37/00, С07Р 213/75, Аб1ТК 31/4965, СО7О 241/18, Аб1Р 29/00 5.2 Другая проверенная документация в той мере, в какой она включена в поисковые подборки: 5.3 Электронные базы данных, использованные при поиске (название базы, и если, возможно, поисковые термины): Езрасепе Соозе эспо]аг, Раеагсв, КОРТО 6. ДОКУМЕНТЫ, ОТНОСЯЩИЕСЯ К ПРЕДМЕТУ ПОИСКА Кате- Наименование документа с указанием (где необходимо) частей, Относится к гория* относящихся к ...

Novel sulfonylurea and herbicidal and / or growth regulating composition

Method of preparing phenylhydrazinopyridazines

Compounds are disclosed of the formula wherein two of R1, R2 and R3 are hydrogen and the third group is hydrogen, lower alkyl, fluoro, chloro, bromo, lower alkoxy, lower alkenyloxy; and R5 is isopropyl or tertiary butyl. These compounds find use as .beta.-adrenergic blocking agents and vasodilators.

Phenylpyridazine derivatives and drugs containing the same

提供一种苯基哒嗪化合物，由下式(I)表示：(其中R 1 代表取代或未取代的苯基或取代或未取代的吡啶基；R 2 代表低级烷氧基、低级烷硫基、低级烷基亚磺酰基或低级烷基磺酰基；R 3 代表氢原子或低级烷氧基；和R 4 代表氢原子或取代的烷基)，所述苯基哒嗪化合物对白细胞间介素－1β的产生有极好的抑制活性，适用于预防和治疗因刺激白细胞间介素－1β产生所引起的疾病，如免疫系统疾病、炎性疾病、和缺血性疾病。

Pyridazinone derivatives, process for their preparation and their use as fungicides

Chemical compounds as inhibitors of amyloid beta protein production

A compound of the formula I in which ##STR1## Z is O or S; R 11 is a halogen atom; R 12 is a halogen atom or a trifluoromethyl group; and X is S, SO, SO 2 , O or NH; R 4 is naphthyl, quinolinyl, benzimidazolyl, pyridyl, pyradazinyl, benzoxazolyl or benzothiazolyl, unsubstituted or substituted by one or two substituents selected from a halogen atom, (1-4C)alkyl, (1-4C)alkoxy, nitro, (1-4C)alkoxycarbonyl, halo(1-4C)alkyl, and phenyl; or a pharmaceutically acceptable salt thereof. The compounds are useful as inhibitors of amyloid beta-protein production.

Substituted 5,6-diphenyl-3(2H)-pyridazinone for use as fungicides

모든 기하 및 입체이성질체를 포함하는 화학식 1 의 화합물, 이의 N -옥사이드 및 염이 개시되어 있다: [화학식 1] 상기 식에서, W, R 1 , R 2 , R 3 , R 4 , R 5 m, n 및 p는 본 개시내용에 정의된 바와 같다. 또한, 화학식 1 의 화합물을 함유하는 조성물, 및 유효량의 화합물 또는 본 발명의 조성물을 적용하는 단계를 포함하는, 진균 병원체에 의해 야기되는 식물 질환을 방제하기 위한 방법이 개시되어 있다.

Patent FR2275213B1

Ror gamma modulators (rorγ)

FIELD: medicine; pharmaceuticals.SUBSTANCE: invention relates to novel compounds of formula I, as well as pharmaceutical compositions based thereon.(formula I)EFFECT: obtaining novel compounds suitable for treating RORγ-mediated diseases or conditions, such as rheumatoid arthritis, psoriasis, inflammatory bowel disease, Crohn's disease and multiple sclerosis.12 cl, 39 ex РОССИЙСКАЯ ФЕДЕРАЦИЯ ФЕДЕРАЛЬНАЯ СЛУЖБА ПО ИНТЕЛЛЕКТУАЛЬНОЙ СОБСТВЕННОСТИ (12) (19) RU (11) (13) 2 733 406 C2 (51) МПК C07D 213/71 (2006.01) C07D 213/75 (2006.01) C07D 241/18 (2006.01) A61K 31/44 (2006.01) A61K 31/4965 (2006.01) A61P 29/00 (2006.01) A61P 37/00 (2006.01) ОПИСАНИЕ ИЗОБРЕТЕНИЯ К ПАТЕНТУ (52) СПК C07D 213/71 (2020.05); C07D 213/75 (2020.05); C07D 241/18 (2020.05); A61K 31/44 (2020.05); A61K 31/4965 (2020.05); A61P 29/00 (2020.05); A61P 37/00 (2020.05) (21)(22) Заявка: 2017145928, 03.06.2016 03.06.2016 Дата регистрации: 01.10.2020 05.06.2015 EP 15170768.4 (43) Дата публикации заявки: 10.07.2019 Бюл. № 19 (56) Список документов, цитированных в отчете о поиске: WO2013029338 A1, 07.03.2013. RU 2519123 C2, 10.06.2014. (45) Опубликовано: 01.10.2020 Бюл. № 28 (86) Заявка PCT: EP 2016/062708 (03.06.2016) C 2 C 2 (85) Дата начала рассмотрения заявки PCT на национальной фазе: 09.01.2018 (87) Публикация заявки PCT: 2 7 3 3 4 0 6 WO 2016/193468 (08.12.2016) R U (73) Патентообладатель(и): ЛИД ФАРМА ХОЛДИНГ Б.В. (NL), САНОФИ (FR) 2 7 3 3 4 0 6 Приоритет(ы): (30) Конвенционный приоритет: R U (24) Дата начала отсчета срока действия патента: (72) Автор(ы): КАЛС, Йосеф Мария Герардус Барбара (NL), МАШНИК, Давид (FR), НАБЮЮРС, Сандер Бернардус (NL), САБЮКО, Жан-Франсуа (FR), ШИО, Лоран (FR) Адрес для переписки: 129090, Москва, ул. Б. Спасская, 25, стр. 3, ООО "Юридическая фирма Городисский и Партнеры" (54) МОДУЛЯТОРЫ ROR ГАММА (RORγ) (57) Реферат: Изобретение относится к новым соединениям формулы I, а также фармацевтическим композициям на их основе. Технический результат: получены новые соединения, ...

Patent FR2335227B1

6-Hydrazino 3- phenyl-pyridazines and salts - with vasodilator and beta-adrenergic blocking activity for treating cardiovascular disorders

Substituted phenyl-2-propenoic acid derivatives and their use as fungicides.

PYRIDAZINE DERIVATIVES AND THEIR APPLICATION AS FUNGICIDES

L'INVENTION A POUR OBJET DES NOUVEAUX DERIVES DE PYRIDAZINES DE FORMULE: (CF DESSIN DANS BOPI) CES COMPOSES SONT UTILISABLES COMME FONGICIDES. THE SUBJECT OF THE INVENTION IS NEW PYRIDAZINE DERIVATIVES OF THE FORMULA: (CF DRAWING IN BOPI) THESE COMPOUNDS CAN BE USED AS FUNGICIDES.

3,5-diphenyl-4-(1h)-pyridazinones (thiones)

Abstract of the Disclosure A series of 3,5-diphenyl-4(1H)-pyridazinones and thiones are useful for reducing the vigor of unwanted herbaceous plants. The compounds are effective when applied either preemergence or postemergence to the unwanted plants. The compounds bear l-alkyl substituents, and the phenyl rings may be substituted as well.

Novel hydroxyphenylketone

6-thioxopyridazine derivatives

Compounds of the formula I in which R1, R2 and R3 have the definitions stated in claim 1 are inhibitors of tyrosine kinases, more particularly of Met kinase, and can be used for purposes including the treatment of tumours.

Insecticide,acaricide,haematocide or/and fungicide

Compound pharmaceutical composition processes to relieve pain and to prepare a compound

Pyridaginones having insecticidal and acaricidal activity

내용없음 No content

Dihydropyridazinones, pyridazinones and related compounds as fungicides

ABSTRACT DIHYDROPYRIDAZINONES, PYRIDAZINONES AND RELATED COMPOUNDS AS FUNGICIDES This invention relates to substituted dihydropyridazinones, pyridazinones and related compounds, of the formula

Patent SE309767B

Fungicide compositions containing oxime-ether derivatives as active ingredient and process for the preparation of the active ingredients

Phenylpyridazine derivatives and drugs containing the same

Compounds of the general formula (I) or salts thereof; and drugs containing the compounds or the salts: (I) [wherein R1 is optionally substituted phenyl , pyridyl, or the like; R2 is lower alkoxy, lower alkylthio, lower alkylsulfinyl, lower alkylsulfonyl, or the like; R3 is hydrogen, lower alkox y, or the like; and R4 is hydrogen, substituted alkyl, or the like]. The compounds exhibit an excellent interleukin 1.szlig. production inhibiting activity and are useful as preventive and therapeutic drugs for immunologic diseases, inflammatory diseases, ischemic disease, and so on.

Antihypertensive pyridazin(2H)-3-ones

Compounds of the formula ##STR1## are useful antihypertensive agents.

Pyridazinones endowed with acaricide and insecticide action

"PYRIDAZINONES ENDOWED WITH ACARICIDE AND INSECTICIDE ACTION" There are described new pyridazinones endowed with acaricide and insecticide action, having general formula (I):

5-oxy-pyridazin-3-one derivatives and herbicidal compositions comprising them

Cephalosporin derivatives.

A cephalosporin derivative of the formula I: < IMAGE > I in which X is < IMAGE > represents one of C-7 acyl groups known in the cephalosporin art, R3 is hydrogen or methoxy, R4 is hydrogen, optionally substituted alkyl or allyl, and R5 is an aromatic heterocyclic ring system which is linked via carbon, and which contains a quaternized nitrogen atom.

HETEROCYCLIC DERIVATIVES THAT INHIBIT THE FACTOR XA

Herbicide

Srodek chwastobójczy, zawierajacy substancje czynna i znane substancje pomocnicze, znamienny tym, ze zawiera jako substancje czynna co najmniej jeden zwiazek o wzorze I, w którym kazdy z symboli Rj i R 2 niezaleznie od siebie oznacza grupe hydroksylowa, atom chlorowca, grupe cyjanowa, grupe nitrowa, grupe aminowa, która ewentualnie moze byc podsta- wiona rodnikiem alkilowym o 1-4 atomach wegla, prostolancuchowy lub rozgaleziony rodnik alkilowy o 1 -10 atomach wegla, który ewentualnie moze byc jedno- lub wielokrotnie podstawiony grupa hydroksylowa, atomem chlo- rowca lub grupa cyjanowa, nadto oznacza prostolancuchowa lub rozgaleziona grupe alkoksylowa o 1-10 atomach wegla, rodnik cykloalkilowy o 5-7 ato- mach wegla, grupe cykloalkoksylowa o 5-7 atomach wegla, rodnik fenylowy, grupe fenoksylowa, grupe alkilotio lub alkilosuifonylowa o 1-4 atomach wegla, kazdy z symboli n i m niezaleznie od siebie oznacza liczby 0, 1, 2 lub 3, przy czym suma n+m stanowi liczbe 1-5, R3 oznacza grupe hydroksylowa, atom chlorowca, grupe -0 C(0 )ZR4 lub -0 C(0 )NR4 R5, przy czym R4 oznacza prostolancuchowy lub rozgaleziony, nasycony lub nienasycony rodnik alki- lowy o 1- 15 atomach wegla, który ewentualnie moze byc podstawiony rodni kiem fenylowym, lub oznacza rodnik fenylowy lub rodnik cykloalkilowy o 5-7 atomach wegla, R5 oznacza prostolancuchowy lub rozgaleziony, nasycony lub nienasycony rodnik alkilowy o 1-15 atomach wegla, który ewentualnie moze byc podstawiony rodnikiem fenylowym, lub oznacza rodnik fenylowy lub rodnik cykloalkilowy o 5-7 atomach wegla, Z oznacza wiazanie pojedyn- cze, atom tlenu lub siarki, a X oznacza atom chlorowca, i/lub jego sole fizjologicznie tolerowane przez rosliny Wzór 1 PL PL

Cyclohexanone compounds and herbicides comprising the same

The present invention provides a compound having an excellent efficacy for controlling weeds. A cyclohexanone compound of the formula (I): wherein m is an integer of 1, 2 or 3; n is an integer of any one of 1 to 5; X represents CH 2, O, S, S(O) or S(O)2; R1 represents a hydrogen atom or a methyl group; R2 and R3 represents a hydrogen atom, a C 1-6 alkyl group and the like; R4 represents a C6-10 aryl group or a five- to six- membered heteroaryl group; G represents a hydrogen atom and the like; Z represents a halogen atom, a cyano group, a nitro group, a phenyl group, a C 1-6 alkyl group and the like; is useful as an active ingredient for herbicides.

Substituted nitrogen containing heterocycles as inhibitors of p38 protein kinase

The present invention relates to inhibitors of p38, a mammalian protein kinase involved cell proliferation, cell death and response to extracellular stimuli. The invention also relates to methods for producing these inhibitors. The invention also provides pharmaceutical compositions comprising the inhibitors of the invention and methods of utilizing those compositions in the treatment and prevention of various disorders.

Dihydropyridazinone and pyridazinone as fungicides

Heterocyclic derivatives which inhibit factor xa

6-Thioxo-pyridazine derivatives

Vanilloid receptor ligands and their use in treatments

Aromatic compounds and pharmaceutical compositions containing the compounds

Hydrazinopyridazines.

Phenylpyridazine compounds and medicines containing the same

Process for the preparation of a novel hydrazine compound and its salts, and products obtained

Process for the preparation of pyridazine derivatives

Substituted 5,6-diphenyl-3(2H)-pyridazinone for use as a fungicide

開示されているのは、式（１）【化１】TIFF2023513239000040.tif45170の化合物（その全ての幾何異性体及び立体異性体、Ｎ－オキシド、並びに塩を含む）であり、式中、Ｗ、Ｒ１、Ｒ２、Ｒ３、Ｒ４、Ｒ５、ｍ、ｎ、及びｐは、本開示で定義された通りである。同様に開示されているのは、式（１）の化合物を含む組成物、並びに真菌病原体による引き起こされる植物病害を防除する方法であって、本発明の化合物又は組成物の有効量を適用することを含む方法である。

Pyridazinone derivatives as thyroid hormone receptor agonists

Provided herein are compounds of the formula (I): as well as pharmaceutically acceptable salts thereof, wherein the sub-stituents are as those disclosed in the specification. These compounds, and the pharmaceutical compositions containing them, are useful for the treatment of diseases such as obesity, hyperlipidemia, hypercholes-terolemia and diabetes and other related disorders and diseases, and may be useful for other diseases such as NASH, atherosclerosis, car-diovascular diseases, hypothyroidism, thyroid cancer and other disor-ders and diseases related thereto.

Dihydropyridazinones, pyridazinones and related compounds as fungicides

This invention relates to substituted dihydropyridazinones, pyridazinones and related compounds, of the formula <IMAGE> wherein A, Q, D and R1 are as defined within, compositions containing these compounds and methods of controlling agricultural and mammalian fungal diseases.

Small molecule inhibitors of the pleckstrin homology domain and methods for using same

Pleckstrin homology domain binding compounds, pharmaceutical compositions including such compounds, and methods for their use are described herein.

Process for preparing derivatives of pyridazinone

Substituted pyridazinyloxy(thio)phenyl ureas and derivatives thereof

Disclosed are novel substituted pyridazinyloxy(thio)phenyl ureas and derivatives thereof. The compounds of the instant invention are useful as herbicides and can be formulated to provide herbicidal compositions.

Method for preparing pyridazine compound

本发明公开了一种由式[1]表示的哒嗪化合物，其可用作植物病害控制剂的活性成分，其可以通过以下步骤制备：通过使由式[4]表示的化合物与由式[5]表示的化合物反应而获得由式[3]表示的化合物；通过使化合物[3]脱保护而获得由式[2]表示的化合物；以及使化合物[2]与氯化试剂反应。

Patent GR851235B

Antiulcer thioamide derivs. - prepd. by treating nitrile or acid amide deriv. with an inorganic sulphide and/or sulphonyl halide

L'invention concerne un thioamide de formule :

Heterocyclic neophane analogue and biocidal compositions

Compounds of the formula (I) and their stereoisomers <IMAGE> (I) wherein A, B, C' and D independently of one another denote CH or N, in which at least one of the symbols A, B, C' or D must correspond to a nitrogen atom, X denotes CH2 or oxygen, R1 denotes a radical bonded to a carbon atom from the series comprising H, trialkylsilyl, halogen, nitro, cyano, alkenyl, alkynyl, amino, cycloalkyl, phenyl, phenxy, alkoxy, alkenyloxy, alkynyloxy, hydroxycarbonyl, alkylthio, cycloalkyloxy, alkylcarbonyl, alkoxycarbonyl, alkenyloxycarbonyl, alkynyloxycarbonyl, halogenoalkyl, alkoxyalkyl, halogenoalkoxy, halogenoalkylthio, halogenoalkoxyalkyl, alkylthioalkyl, alkoxyalkoxy, halogenoalkoxyalkoxy, alkenyloxyalkoxy, halogenoalkenyloxy, alkoxyalkylthio, alkylthioalkoxy, alkylthioalkylthio, halogenoalkoxycarbonyl, halogenoalkenyloxycarbonyl or dialkylamino or two radicals R1 when they are positioned ortho to one another together denote a methylenedioxy, ethylenedioxy or alkylene radical, R2 and R3 independently of one another denote alkyl, alkenyl or phenyl, or R2 and R3 denote an alkylene chain which-together with the quaternary carbon atom-forms an unsubstituted or fluorinesubstituted ring having three to six ring members, R4 denotes -H, F, -CN, -CCl3, -C 3BOND CH, (C1-C4)alkyl, -C-NH2, S R5 denotes pyridyl, furyl or thienyl which can all be substituted, phthalimidyl, dialkylmaleimidyl, thiophthalimidyl, dihydrophthalimidyl, tetrahydrophthalimidyl or substituted phenyl, or R4 and R5-together with the carbon atom bridging them-denote an optionally substituted indanyl, cyclopentenoyl or cyclopentenyl radical and n denotes 0, 1 or 2, possess advantageous properties for combating pests, in particular insects and acarids. Furthermore, processes for the preparation of compounds of the formula I are described.

Vanilloid receptor ligands and their use in treatments

Compounds having the general structure formula (I) and compositions containing them, for the treatment of acute, inflammatory and neuropathic pain, dental pain, general headache, migraine, cluster headache, mixed-vascular and non-vascular syndromes, tension headache, general inflammation, arthritis, rheumatic diseases, osteoarthritis, inflammatory bowel disorders, inflammatory eye disorders, inflammatory or unstable bladder disorders, psoriasis, skin complaints with inflammatory components, chronic inflammatory conditions, inflammatory pain and associated hyperalgesia and allodynia, neuropathic pain and associated hyperalgesia and allodynia, diabetic neuropathy pain, causalgia, sympathetically maintained pain, deafferentation syndromes, asthma, epithelial tissue damage or dysfunction, herpes simplex, disturbances of visceral motility at respiratory, genitourinary, gastrointestinal or vascular regions, wounds, burns, allergic skin reactions, pruritus, vitiligo, general gastrointestinal disorders, gastric ulceration, duodenal ulcers, diarrhea, gastric lesions induced by necrotising agents, hair growth, vasomotor or allergic rhinitis, bronchial disorders or bladder disorders.

Arylpyridazinones as prostaglandin endoperoxide H synthase biosynthesis inhibitors

本发明描述了为环加氧酶(COX)抑制剂、特别是环加氧酶-2(COX/2)选择性抑制剂的哒嗪酮化合物，COX-2为与炎症有关的可诱导同种型，与组成同种型环加氧酶-1(COX-1)相反，COX-1在包括胃肠(GI)道和肾脏在内的许多组织内为重要的“管家”酶。用于COX-2的这些化合物的选择性最大限度地减小用目前市售的非甾体抗炎药(NSAID)观察到的不想要的GI和肾副作用。

Soluble epoxide hydrolase inhibitors

Disclosed are sulfone compounds and compositions that inhibit soluble epoxide hydrolase (sEH), methods for preparing the compounds and compositions, and methods for treating patients with such compounds and compositions. The compounds, compositions, and methods are useful for treating a variety of sEH mediated diseases, including hypertensive, cardiovascular, inflammatory, pulmonary, and diabetes-related diseases.

A kind of methyl aryl thio-ether type compounds and its synthetic method and application

本发明公开了一种式(2)所示的甲基芳基硫醚类化合物及其合成方法和应用，在反应溶剂中，以芳基卤化物或芳基类卤化物，与碳酸二甲酯及硫代乙酸钾为反应原料，在金属钯催化剂作用下，在配体、碱的作用下，反应得到所述甲基芳基硫醚类化合物。本发明合成方法反应条件温和，原料价廉易得，反应操作简单，产率较高。本发明合成的甲基芳基硫醚类化合物可为多种天然产物和药物的合成提供关键的骨架结构，可以广泛适用于工业化规模生产。

Heterocyclic derivatives which inhibit factor xa

Heterocyclic neophane analogs, processes for their preparation and their use as pest-combating agents

Compounds of the formula (I) and their stereoisomers (I) wherein A, B, C' or D independently of one another denote CH or N, in which at least one of the symbols A, B, C' or D must correspond to a nitrogen atom, X denotes CH2 or oxygen, R1 denotes a radical bonded to a carbon atom from the series comprising H, trialkylsilyl, halogen, nitro, cyano, alkenyl, alkynyl, amino, cycloalkyl, phenyl, phenoxy, alkoxy, alkenyloxy, alkynyloxy, hydroxy-carbonyl, alkylthio, cycloalkyloxy, alkylcarbonyl, alkoxycarbonyl, alkenyloxycarbonyl, alkynyloxy-carbonyl, halogenoalkyl, alkoxyalkyl, halogenoalkoxy, halogenoalkylthio, halogenoalkoxyalkyl, alkylthio-alkyl, alkoxyalkoxy, halogenoalkoxyalkoxy, alkenyl-oxyalkoxy, halogenoalkenyloxy, alkoxyalkylthio, alkylthioalkoxy, alkylthioalkylthio, halogenalkoxy-carbonyl, halogenoalkenyloxycarbonyl or dialkyl-amino or two radicals R1 when they are positioned ortho to one another together denote a methylene-dioxy, ethylenedioxy or alkylene radical, R2 and R3 independently of one another denote alkyl, alkenyl or phenyl, or R2 and R3 denote an alkylene chain which - together with the quaternary carbon atom-forms an unsubstituted or fluorinesubstituted ring having three to six ring members, R4 denotes -H, F, -CN, -CCl3, -C?CH, (C1-C4)alkyl, -C-NH2, S R5 denotes pyridyl, furyl or thienyl which can all be substituted, phthalimidyl, dialkylmaleimidyl, thio-phthalimidyl, dihydrophthalimidyl, tetrahydro-phthalimidyl or substituted phenyl, or R4 and R5 - together with the carbon atom bridging them - denote an optionally substituted indanyl, cyclo-pentenoyl or cyclopentenyl radical and n denotes 0, 1 or 2, possess advantageous properties for combating pests, in particular insects and acarids. Furthermore, processes for the preparation of compounds of the formula I are described.

Pyridazinone herbicides

New pyridazine derivatives and drugs containing these as effective ingredients

Phenylpyridazine derivatives and drugs containing the same

Phenylpyridazine compounds represented by the following formula (I): <CHEM> (wherein R1 represents a substituted or unsubstituted phenyl or a a substituted or unsubstituted pyridyl; R2 represents a lower alkoxy group, a lower alkylthio group, a lower alkylsufinyl group or a lower alkylsulfonyl group; R3 represents a hydrogen atom or a lower alkoxy group; and R4 represents a hydrogen atom or a substituted alkyl group), are provided having excellent inhibitory activity against interleukin-1 beta production, and useful in the treatment of prevention of diseases caused by stimulation of interleukin-1 beta production, such as immune system diseases, inflammatory diseases, and ischemic diseases.

Method for producing pyridazinone compounds and intermediate thereof

본 발명은 하기 반응식에 나타낸 바와 같이 피리다지논 화합물 및 그 중간체의 신규한 제조 방법에 관한 것이다: [식 중, 기호는 명세서에 정의된 바와 같음]. The present invention relates to a novel process for preparing pyridazinone compounds and their intermediates as shown in the following reaction schemes: Wherein the symbols are as defined in the description.

Pyridazinone derivatives

Pyridazinone derivatives of the formula <IMAGE> (I) where R1 is alkyl, alkenyl, cycloalkyl or unsubstituted or substituted phenyl, R2 is chlorine or bromine, R3 is hydrogen, alkyl, cycloalkyl or unsubstituted or substituted phenyl and X is SO or SO2, with the proviso that R1 is not methyl when X is SO2, R2 is chlorine and R3 is phenyl, and fungicides containing these compounds.

Novel pyridazine derivatives and drugs containing the same as the active ingredient

본 발명은 식(1) The present invention is formula (1) (식중, R l 은 (치환)아릴기, R 2 는 4 위치에 저급 알콕시실기, 저급알킬티오기 등이 치환된 페닐기, R 3 는 H, 저급알콕실기, 할로겐화 저급알킬기, 저급시클로알킬기, (치환)아릴기, (치환)아릴옥시기, (치환)질소함유복소환잔기, (치환)아미노카르보닐기, 또는 저급알킬카르보닐기, A는 단결합 또는 저급알킬렌기 또는 저급알케닐렌기, X는 O 또는 S, 파선은 4 위치와 5 위치의 탄소간 결합이 단결합 또는 이중결합인 것을 나타낸다)으로 표시되는 피리다진 유도체 또는 그 염 및 이를 유효성분으로 하는 의약에 관한 것이다. 이 화합물은 우수한 인터로이킨-1β 생산억제작용을 가지며, 면역계 질환, 염증성 질환, 허혈성 질환 등의 예방 또는 치료제로서 유용하다. (Wherein R 1 is a (substituted) aryl group, R 2 is a phenyl group substituted with a lower alkoxyl group, a lower alkylthio group, etc. at the 4 position, R 3 is H, a lower alkoxyl group, a halogenated lower alkyl group, a lower cycloalkyl group, ( Substituted) aryl group, (substituted) aryloxy group, (substituted) nitrogen-containing heterocyclic residue, (substituted) aminocarbonyl group, or lower alkylcarbonyl group, A is a single bond or lower alkylene group or lower alkenylene group, X is O or S, a broken line indicates a pyridazine derivative or a salt thereof represented by 4) and a 5-position carbon bond is a single bond or a double bond) and a medicament using the same as an active ingredient. This compound has excellent interleukin-1β production inhibitory action and is useful as a prophylactic or therapeutic agent for immune system diseases, inflammatory diseases, ischemic diseases and the like.

Aromatic compounds and pharmaceutical compositions containing them

The invention relates to compounds of formula (I), wherein A is an optionally substituted, ring system provided that the -CH(R?3)N(R2)B-R1¿ and -OD groups are positioned in a 1,2 relationship to one another on ring carbon atoms and the ring atom positioned ortho to the -OD linking group (and therefore in the 3-position relative to the -CHR3NR2- linking group) is not substituted; B is an optionally substituted ring system; R1 is positioned on ring B in a 1,3 or 1,4 relationship with the -CH(R3)N(R2)- linking group and is as defined in the description; R2 is hydrogen, C¿1-6?alkyl, optionally substituted by hydroxy, cyano or trifluoromethyl, C2-6alkenyl (provided the double bond is not in the 1-position), (C2-6alkynyl (provided the triple bond is not in the 1-position), phenylC1-3alkyl or pyridylC1-3alkyl; R?3¿ is hydrogen, methyl or ethyl; D is hydrogen, an optionally substituted 5-7 membered carbocyclic ring containing one double bond, C¿1-3?alkyl substituted by an optionally substituted 5-7 membered carbocyclic ring containing one double bond or D is of the formula -(CH2)nCH(R?4)C(R5)=C(R6)R7¿ and N-oxides of -NR2 where chemically possible; and S-oxides of sulphur containing rings where chemically possible; and pharmaceutically acceptable salts and in vivo hydrolysable esters and amides thereof; excluding 4-[5-carboxy-2-hydroxybenzylamino]benzoic acid, 4-[2,5-dihydroxybenzylamino]benzoic acid, 5-[2-hydroxybenzylamino]-2-hydroxybenzoic acid, 3-[2,5-dihydroxybenzylamino]benzoic acid, 4-[2,5-dihydroxybenzylamino]benzenecarboxamide, 3-[2-hydroxybenzylamino]benzoic acid, 4-[2,5-dihydroxybenzylamino]-2-hydroxybenzoic acid, 4-[hydroxybenzylamino]-2-hydroxybenzoic acid and 4[2-hydroxybenzylamino]benzoic acid. Processes for their preparation, intermediates in their preparation, their use as therapeutic agents and pharmaceutical compositions containing them.

Process for the preparation of herbicidally active pyridazine derivatives