ПРОЛЕКАРСТВЕННЫЕ СРЕДСТВА ИНГИБИТОРОВ ОБРАТНОЙ ТРАНСКРИПТАЗЫ ВИЧ

FIELD: chemistry. SUBSTANCE: invention relates to a novel compound of formula I or a pharmaceutically acceptable salt thereof. In formula I R 1 is ; R 2 is halogen or -C 1-3 -alkyl substituted with 1–3 -F; R 3 is (a) halogen, (b) -C 1-3 -alkyl substituted with 1-3 -F, or (3) phenyl substituted with halogen; and R 4 is , or , where X + are an alkali metal ion. EFFECT: compounds have HIV-1 reverse transcriptase inhibitor properties and can be used for treating or preventing HIV infection or treating, preventing or delaying onset of AIDS. 12 cl, 3 tbl, 8 ex РОССИЙСКАЯ ФЕДЕРАЦИЯ (19) RU (11) (13) 2 693 622 C2 (51) МПК C07F 9/6558 (2006.01) A61K 31/662 (2006.01) A61P 31/18 (2006.01) ФЕДЕРАЛЬНАЯ СЛУЖБА ПО ИНТЕЛЛЕКТУАЛЬНОЙ СОБСТВЕННОСТИ (12) ОПИСАНИЕ ИЗОБРЕТЕНИЯ К ПАТЕНТУ (52) СПК C07F 9/6558 (2019.02); A61K 31/662 (2019.02); A61P 31/18 (2019.02) (21)(22) Заявка: 2016142611, 27.03.2015 (24) Дата начала отсчета срока действия патента: Дата регистрации: 03.07.2019 (73) Патентообладатель(и): МЕРК ШАРП И ДОУМ КОРП. (US) (56) Список документов, цитированных в отчете о поиске: US 2013296382 A1, 07.11. 2013. US 01.04.2014 US 61/973,689 (43) Дата публикации заявки: 03.05.2018 Бюл. № 13 (45) Опубликовано: 03.07.2019 Бюл. № 19 (85) Дата начала рассмотрения заявки PCT на национальной фазе: 01.11.2016 US 2015/022868 (27.03.2015) C 2 C 2 (86) Заявка PCT: 2005215554 A1, 29.09.2005. WO 2014058747 A1, 17.04.2014. Lei Ji; et al., Synthesis and AntiHIV-1 Activity Evaluation of 5-Alkyl-2alkylthio-6-(arylcarbonyl or αcyanoarylmethyl)-3,4-dihydropyrimidin-4(3 H )-ones as Novel Non-nucleoside HIV-1 Reverse Transcriptase Inhibitors, Journal of Medicinal Chemistry, 2007, (см. прод.) (87) Публикация заявки PCT: WO 2015/153304 (08.10.2015) 2 6 9 3 6 2 2 2 6 9 3 6 2 2 Приоритет(ы): (30) Конвенционный приоритет: R U R U 27.03.2015 (72) Автор(ы): БЕРГИ Кристофер С. (US), ФРИЦЕН Джеффри Ф. (US), БАЛСЕЛЛС Хауме (US), ПАТЕЛ Мехул (US) Адрес для переписки: 129090, Москва, ул. Б.Спасская, 25, строение 3, ...

ПРОИЗВОДНЫЕ 3(2Н)-ПИРИДАЗИНОНОВ ИЛИ ИХ ФАРМАЦЕВТИЧЕСКИ ПРИЕМЛЕМЫЕ АДДИТИВНЫЕ СОЛИ КИСЛОТЫ И ФАРМАЦЕВТИЧЕСКАЯ КОМПОЗИЦИЯ НА ИХ ОСНОВЕ

Представлено новое 3(2Н) -пиридазиноновое производное формулы I, где R1 представляет атом водорода или С1-4-алкил; каждый R2 и R3 представляет атом водорода; Х представляет атом хлора или атом брома; Y1 представляет атом водорода, атом галогена, нитрогруппу или С1-4-алкоксигруппу; Y2 представляет С1-4- алкоксигруппу; А представляет С1-5-алкиленовую цепь, которая может быть замещена гидроксильной группой; В представляет карбонильную группу или метиленовую цепь, которая может быть замещена С1-4-алкильной группой; а) R4 представляет атом водорода, R5 представляет Z-Ar, где Z представляет собой С1-5 -алкиленовую цепь, а Ar представляет пиридил, либо в) R4 и R5, взятые вместе со смежным атомом азота, образуют 4-замещенное пиперазиновое кольцо формулы II, где R6 представляет собой С1-4-алкильную группу, которая может быть замещена фенильной группой, которая может быть замещена Y3, где Y3 является атомом галогена, аминогруппой, N-формиламиногруппой или С1-4-алкилкарбониламиногруппой; пиридилом ...

БЕНЗИЛПИРИДАЗИНОНЫ, КАК ИНГИБИТОРЫ ОБРАТНОЙ ТРАНСКРИПТАЗЫ

... 1. Соединение формулы I в которой X1 выбран из группы, включающей R5O, R5S(O)n, R5CH2, R5CH2O, R5CH2S(O)n, R5OCH2, R5S(O)nCH2 и NR5R6; R1 и R2 обозначают (i) заместители, независимо выбранные из группы, включающей водород, C1-С6алкил, C1-С6галогеналкил, С3-С8циклоалкил, C1-С6алкоксигруппу, C1-С6алкилтиогруппу, C1-С6алкилсульфинил, C1 -С6сульфонил, C1-С6галогеналкоксигруппу, C1-С6галогеналкилтиогруппу, галоген, аминогруппу, алкиламиногруппу, диалкиламиногруппу, аминоацил, нитрогруппу и цианогруппу; или (ii) взятые совместно обозначают -СН=СН-СН=СН-, или (iii) взятые совместно с атомами углерода, к которым они присоединены, образуют 5- или 6-членное гетероароматическое или гетероциклическое кольцо, содержащее 1 или 2 гетероатома, независимо выбранные из группы, включающей О, S и NH; R3 выбран из группы, включающей водород, C1-С6алкил, С1-С6галогеналкил, С3-С8циклоалкил, C1-С6алкилтиогруппу, С1-С6галогеналкилтиогруппу, галоген, аминогруппу, алкиламиногруппу, диалкиламиногруппу, аминоацил, ...

ПРОИЗВОДНЫЕ ГЕТЕРОАРИЛ-ЗАМЕЩЕННОГО АМИНОЦИКЛОДЕКАНА

... 1. Соединения формулы (I) где U означает О или свободную электронную пару, V означает простую связь, О, S, -СН=СН-СН2-O-, -СН=СН- или -С≡С-, m и n независимо друг от друга равны 0-7 и m+n равно 0-7, при условии, что m не равно 0, если V означает О или S, о равно 0-2, А1 означает водород, (низш.)алкил, гидрокси(низш.)алкил или (низш.)алкенил, А2 означает (низш.)алкил, циклоалкил, циклоалкил(низш.)алкил или (низш.)алкенил, необязательно замещенный R1, или А1 и А2 связаны друг с другом с образованием цикла и -А1-А2 - означает (низш.)алкилен или (низш.)алкенилен, необязательно замещенный R1, в котором одна из -СН2 - групп в составе -А1-А2 - необязательно замещена группой NR2, S или О, А3 и А4 независимо друг от друга означают водород или (низш.)алкил, или А3 и А4 связаны друг с другом и вместе с атомом углерода, к которому они присоединены, образуют цикл, а -А3-А4 - означает -(СН2 )2-5-, А5 означает водород, (низш.)алкил или (низш.)алкенил, А6 означает пиридинил, пиридазинил, пиримидинил или ...

Способ получения пиридазинил-гидразонов или их кислотно-аддитивных солей

Pyridazinylhydrazones capable of lowering blood pressure having the formula <IMAGE> wherein R1 is hydrogen, chlorine, alkyl having from 1 to 4 carbon atoms, methoxy, hydroxyl, carbamoyl or cyano; R2 is morpholino; and K is a group having the formula <IMAGE> wherein one of R3, R4, R5 or R6 is carboxyl or alkoxycarbonyl.

Способ получения пиридазинилгидразонов или их солей с кислотами

Pyridazinylhydrazones capable of lowering blood pressure having the formula <IMAGE> wherein R1 is hydrogen, chlorine, alkyl having from 1 to 4 carbon atoms, methoxy, hydroxyl, carbamoyl or cyano; R2 is morpholino; and K is a group having the formula <IMAGE> wherein one of R3, R4, R5 or R6 is carboxyl or alkoxycarbonyl.

Гербицидный состав

Способ получения замещенных основанием пиридазинов или их солянокислых солей

... 1. Способ получевиязамещенных основанием пиридазинов общей формулы I Y 0-СНгСН-СНг-Ш-сНг-СНг Н-1 А , ОН где R , R , R - независимо друг от друга водород, низший алкил, низший а л ко к сил или аллилоксил, W Y водород, солей, о тили их солянокислых тем, что замеличающийся щенный основанием пиридазин общей формулы I, где R , R , R имеют указанные значения-, W - хлор или бром-, Y - водород или гидролитически отщепляющийся остаток - бензил, алкил-, алкокси- или хлорбензил, гидрируют в растворителе или диспергаторе в присутствии катализатора гидрирования с применением водороСО да. 2.Способ ПОП.1, отличающий с я тем, что используют соединение формулы I, где Y - водород . 3.Способ по п.1 и 2, о т л ичающийся тем, что используют соединение, где только один из заместителей R , R , R имеет значение, отличное от водорода.

Способ выделения 5-амино-4-хлор-2-фенил-3/2 @ /-пиридазинона

Способ борьбы с нежелательными растениями

Die vorliegende Anmeldung betrifft neue wertvolle Pyridazone-(6) mit guter herbizider Wirkung, Herbizide, die diese Verbindungen enthalten, und Verfahren zur Bekämpfung unerwünschten Pflanzenwuchses mit diesen Verbindungen.

GLUKOKINASE AKTIVATOREN

BASIC SUBSTITUTED PYRIDAZINES, THEIR PREPARATION AND THEIR USE

Wasserloesliche Mischungen von Sulfonamid- und Tetracyclin-Saeuresalzen

5-AMINO - 4 - CHLORO - 2 - PHENYL - 3 - (2H) - PYRIDAZINONE FREE FROM 5-CHLORO-4-AMINIO-2-PHENYL - 3(2H) - PYRIDAZIOE AS A SELECTIVE WEED KILLER

Acylated sulfapyridazines

The invention comprises sulpha-pyridazines of the formula wherein R is hydrogen, halogen or an alkyl or alkoxy radical of 1-6 carbon atoms and R1 is an alkanoyl radical, e.g. acetyl, propionyl, butyryl, valeryl or caproyl, and their preparation either by reacting a pyridazine compound of the formula wherein X is nitro or carbobenzyloxyamino and Y is hydrogen or an alkali-metal, with an alkanoic acid anhydride or alkanoyl chloride and hydrogenating the resulting intermediate carbobenzyloxy or nitro derivative, or by reacting a compound of the formula with an alkanoic acid anhydride. 3-(N4-Benzyloxycarbonyl - sulphanilamido) - 6 - methoxypyridazine is made by the action of carbobenzyloxy-chloride on 3-sulphanilamido -6-methoxypyridazine.ALSO:Pharmaceutical preparations having anti-bacterial activity comprise N1-acylated pyridazines of the formula wherein R is hydrogen, halogen, or a lower alkyl or alkoxy ...

Substituted pyridazones and plant-treating compositions containing them

The invention comprises substituted pyridazones of formula in which A denotes a hydrogen atom, B denotes a hydroxyl group, or A and B together denote an oxo radical (= o), R denotes a hydrogen atom, a linear or branched alkyl group, a linear or branched halogensubstituted alkyl group, a halogen-substituted phenoxy- or an alkylhalo-phenoxy-alkyl group, an alkenyl group, an aralkyl group, the group when A and B together represent an oxo radical, a phenyl group or a halogen-substituted phenyl group, and D denotes a phenyl group or a cycloalkyl group. The compounds can be prepared by reacting aminopyridazones of formula with aldehydes, carboxylic acids or carboxylic acid derivatives having the formula RCOX in which R has the meaning given above and X is H, Cl, Br, OH or the group -OCOR. For example, 1-phenyl-4-chloroacetyl-amino-5-chloropyridazone-6 is obtained by treating the corresponding 4-amino compound with chloroacetyl ...

Inhibition of the replication of HIV and related viruses using thiourea derivative compounds or salts thereof.

Method of aids, inhibition of the replication of hiv by contacting hiv with a compound of the formula-(see file) ...

Inhibition of the replicateion of HIV and related viruses using thiourea derivative compounds or salts thereof.

Method for inhibiting the replication of hiv by contacting hiv with a compound of the formula: ...

COMPOUNDS AND METHODS FOR INHIBITION OF HIV AND RELATED VIRUSES

Inhihition of the replication of hiv and related viruses using thiourea derivative compounds or salts thereof

Biaryl amide compounds as kinase inhibitors

Pyridazinone compounds and their use as DAAO inhibitors

New derivatives of the active methyl-4 phényl-6 pyridazin on the central nervous system.

Weedkiller containing a dioxide of benzothiadiazinone substituted and another active ingredient.

COMPOUNDS AND METHODS FOR INHIBITION OF HIV AND RELATED VIRUSES

Pyridazinone compounds and their use as DAAO inhibitors

Pyridazinone compounds and their use as DAAO inhibitors

Biaryl amide compounds as kinase inhibitors

Inhihition of the replication of hiv and related viruses using thiourea derivative compounds or salts thereof

COMPOUNDS AND METHODS FOR INHIBITION OF HIV AND RELATED VIRUSES

Biaryl amide compounds as kinase inhibitors

VERFAHREN ZUR HERSTELLUNG NEUER PYRIDAZINY -HYDRAZON-DERIVATE UND DER PHYSIOLOGISCHEN VERTRAEGLICHEN SAEUREADDITIONS-SALZE DIESER VERBINDUNGEN

3-HETEROCYCLYL-SUBSTITUIERTE of BENZOIC ACID DERIVATIVES

PROCEDURE FOR the PRODUCTION OF 4,5-DICHLOR-2PHENYL-3 (2H) - PYRIDAZINON FROM 4-AMINO-5-CHLOR-2 PHENYL-3 (2H) - PYRIDAZINON

PROCEDURE FOR THE PRODUCTION OF NEW PYRIDAZINYL - HYDRAZON DERIVATIVES AND THE PHYSIOLOGICALLY COMPATIBLE ONES OF ACID ADDITION SALTS OF THESE CONNECTIONS

PROCEDURE FOR the PRODUCTION OF 4-AMINO-5-CHLOR-1 PHENYLPYRIDAZINON

FOR THE TREATMENT OF THROMBOTI SUFFERING APTITUDE UREA ANTAGONIST OF THE P2Y1REZEPTORS

PYRIDAZINDERIVATE AND YOUR USE AS THERAPEUTIC ACTIVE SUBSTANCES

CARBONIC ACID DERIVATIVES, THE CONNECTION OF INTEGRINEN TO ITS RECEPTORS RESTRAINING

ANTI-IGNITING 4-AMINOPHENOL-DERIVATE.

BASIC PYRIDAZINE, YOUR PRODUCTION AND YOUR USE SUBSTITUTED.

ANTIHYPERTENSIVA.

SUBSTITUTED PYRIDAZONE, PROCEDURES FOR IHERER PRODUCTION AND YOUR APPLICATION AS HERBICIDES

3 (3 ' - AMINO-2' HYDROXY-N-PROP-1' OXY) - 6ISOPROPYLIDENHYDRAZINOPYRIDAZINE, PROCEDURE TOO THEIR PRODUCTION AND THESE CONNECTIONS CONTAINING DRUGS.

DIHYDROPYRIDAZINONE.

4-METHYL-6-PHENYL-PYRIDAZINDERIVATE WITH an EFFECT ON the CENTER the NERVOUS SYSTEM.

PYRIDAZINON DERIVATIVES, MANUFACTURING PROCESSES AND USE

Herbicide

Procedure for the production of new Pyridazinderivaten and of their acid addition salts

PROCEDURE FOR PRODUCTION OF 3 (2H) PYRIDAZINON-4 SUBSTITUTED AMINO-5-CHLORO of DERIVATIVES

BIPHENYLDERIVATE AND YOUR USE AS ACTIVATORS OF THE PPAR GAMMA RECEPTOR

PYRIDAZINON DERIVATIVES

Procedure for the production of pure 5-Amino-4-chlor-2-phenylpyridazin-3-on

Herbicide means

Herbicides mixture

Herbicides mixture

Procedure for the production of new 6-Alkoxy-pyridaziniumverbindungen

SUBSTITUTED ALKYLAMINOPYRIDAZINONDERIVATE, PROCEDURES FOR YOUR PRODUCTION AND THESE CONTAINING PHARMACEUTICAL PREPARATIONS

Substituted carbonucleoside derivatives useful as anticancer agents

Compounds of the general formula : processes for the preparation of these compounds, compositions containing these compounds, and the compounds for use in treating cancer.

SUBSTITUTED-3-OXO-1,4-DIAZINES

BENZOYL UREA DERIVATIVES

HETEROCYCLIC SUBSTITUTED 4-AMINO PHENOL DERIVATIVES

Amine derivative having NPY Y5 receptor antagonist activity

Pyridazine derivatives and their use as therapeutic agents

Phenol derivatives and pharmaceutical or cosmetic use thereof

The invention relates to novel compounds having formula (I) and the cosmetic or pharmaceutical use thereof.

Biphenyl derivatives and their use as PPAR-GAMMA receptor activators

Pyridazine derivatives manufacturing method and related composition

Substituted alkylaminopyridazinone derivatives, process for the preparation thereof and pharmaceutical composition containing the same

Novel heterocyclic compounds as bromodomain inhibitors

The present disciosure relates to compounds, which are useful for inhibition of BET protein function by binding to bromodomains, and their use in therapy.

N-(heteroaryl)-sulfonamide derivatives useful as S100-inhibitors

A compound of formula (I), or a pharmaceutically acceptable salt thereof and a pharmaceutical composition comprising the compound. The compound is an inhibitor of interactions between S100A9 and interaction partners such as RAGE, TLR4 and EMMPRIN and as such is useful in the treatment of disorders such as cancer, autoimmune disorders, inflammatory disorders and neurodegenerative disorders.

Method for producing 4-amino-5-chloro-1-phenyl pyridazinone-(6)

3,4-DI-SUBSTITUTED PYRIDAZINEDIONES AS CXC CHEMOKINE RECEPTOR ANTAGONISTS

Disclosed compounds of the formula (I) or a pharmaceutically acceptable salt or solvate thereof. The compounds are useful for the treatment of chemokine- mediated diseases such as acute and chronic inflammatory disorders and cancer.

DIHYDROPYRIDAZINONE DERIVATIVES

... 11826 Compounds of the formula (I) : (I) and pharmaceutically acceptable salts are described, wherein R1 is hydrogen or methyl and R2 is hydrogen or C1-4alkyl. These compounds have inotropic, vasodilator, bronchodilating and platelet aggregation inhibiting properties. Pharmaceutical compositions are described as are methods of use. Intermediates and processes for the preparation of the compounds of the formula (I) are descibed.

PROCESS FOR OBTAINING 4,5-DICHLORO-2-PHENYL-3(2H)- PYRIDAZINONE FROM 5-CHLORO-4-AMINO-2-PHENYL-3(2H) - PYRIDAZINONE

A process for obtaining 4,5-dichloro-2-phenyl-3(2H)-pyridazinone from 5-chloro-4-amino-2-phenyl-3(2H)-pyridazinone. According to this process, 5-chloro-4-amino-2-phenyl-3(2H) pyridazinone is first diazotized to give the following compound of formula (I): (I) This compound of formula (1) is then recovered by dilution with water and filtration. In a second stage, the so-recovered compound of formula (I) is reacted with thionyl chloride in accordance with the following reaction: (I) The resulting 4,5-dichloro-2-phenyl-3(2H)-pyridazinone is finally recovered by dilution with water and filtration.

PYRIDAZONE DERIVATIVES

3(2H)PYRIDAZINONE, PROCESS FOR ITS PREPARATION AND ANTI-ALLERGIC AGENT CONTAINING IT

A 3(2H)pyridazinone of the formula: (I) wherein R1 is hydrogen or C1-C5 alkyl; R2 is hydrogen, C1-C8 alkyl, chlorine or bromine; A is -NR3- or -O-; X is (CH2)n-, -CH(OR4)-, -CO- or a single bond; when X is -(CH2)n- or a single bond, B is O-, -S-, -NH-, -OSO2-, or -OCO- or a single bond, when X is -CH(OR4)-, B is -O-, -S-, -NH- or OSO2-, and when X is -CO-, B is -O- or -S-; and each of Y1, Y2 and Y3 which may be the same or different, is hydrogen, C1-C8 alkyl, C2-C8 alkenyl, halogen, -OR5, -CO2R6, CH=CHCO2R7, , -CON(R8)(R9), -COR10, or two of Y1, Y2 and Y3 together form , and a pharmaceutically acceptable salt thereof. Compounds of the formula (I) as defined above are useful for reducing the incidence or severity of an allergy induced in a subject by SRS-A.

3(2H)PYRIDAZINONE, PROCESS FOR ITS PREPARATION AND ANTAGONISTIC AGENT AGAINST SRS-A CONTAINING IT

A 3(2H)pyridazinone of the formula: (I) wherein R1 is hydrogen, 2-propenyl or straight chained or branched C1-C4 alkyl; R2 is hydrogen or C1-C3 alkyl; X is chlorine or bromine; Y is hydrogen, nitro, -NHR3 wherein R3 is hydrogen or straight chained or branched C1-C4 alkyl, -AR4 wherein A is oxygen or sulfur and R4 is hydrogen, straight chained or branched C1-C6 alkyl, C3-C6 alkenyl having one double bond, C3-C6 alkynyl having one triple bond, phenyl or wherein R5 is hydrogen or C1-C4 alkyl, or halogen: Z1 is hydrogen, C1-C4 alkyl, -OR6 wherein R6 is hydrogen, straight chained or branched C1-C8 alkyl or wherein n is an integer of from 1 to 4, -N(R7)2 wherein R7 is C1-C4 alkyl, or halogen; Z2 is C1-C4 alkyl, -OR6 wherein R6 is as defined above, -N(R7)2 wherein R7 is as defined above, or halogen, provided that when R1 is straight chained or branched C2-C4 alkyl, Y is not hydrogen and when R1 is hydrogen, methyl or 2-propenyl, Y and R2 are not simultaneously hydrogen, or a ...

3(2H)PYRIDAZINONE, PROCESS FOR ITS PREPARATION AND ANTI-ALLERGIC AGENT CONTAINING IT

6-OXO-1,6-DIHYDROPYRIDAZINE DERIVATIVE, PREPARATION METHOD THEREFOR AND MEDICAL USE THEREOF

A 6-oxo-1,6-dihydropyridazine derivative, a preparation method therefor and medical use thereof, in particular, a 6-oxo-1,6-dihydropyridazine derivative represented by general formula (I), a preparation method therefor, and a pharmaceutical composition containing the derivative, and use thereof as a NaV inhibitor and use thereof in the preparation of a drug for the treatment and/or prevention of pain and pain-related diseases. Each substituent in general formula (I) is the same as defined in the description.

SULFONYLUREAS AND RELATED COMPOUNDS AND USE OF SAME

The present invention relates to compounds of formula (I), and pharmaceutically acceptable salts, solvates and prodrugs thereof: Formula (I) wherein Q is selected from O, S and Se; J is S or Se; W1 and W2, when present, are independently selected from N and C; R1 and R2 are independently selected from the group consisting of hydrogen, C1-C12alkyl, C2-C12alkenyl, C2-C12alkynyl, aryl, heterocyclyl, heteroaryl, cycloalkyl, cycloalkenyl, amino, amido, alkylthio, acyl, arylalkyl and acylamido, all of which may be optionally substituted; and wherein at least one of W1 and W2 is present and is a nitrogen atom and when R1 and R2 are cyclic then the respective W1 or W2 may form part of the ring structure. The present invention also relates to pharmaceutical compositions including such compounds, to methods of treatment using such compounds, in particular in relation to NLRP3 inflammasome mediated disorders, and to associated diagnostic uses.

PYRIDAZONE DERIVATIVES

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.

BENZAMIDE DERIVATIVES AS P2X7 RECEPTOR ANTAGONISTS

The invention relates to benzamide derivatives of formula (I),wherein R1, R2, R3, R4, R5, R6, n and Y are as defined in the description, their preparation and their use as pharmaceutically active compounds.

PYRIDAZINONE DERIVATIVES

Disclosed are a 3(2H)-pyridazinone derivative of the formula (I) or its salt, a process for its production and a pharmaceutical composition containing thereof: (see formula I) (wherein R1, R2 and R3 are each hydrogen C1-4 alkyl, X is chlorine or bromine, Y1 is hydrogen, halogen, nitro, amino or C1-4 alkoxy, Y2 is hydrogen, halogen, hydroxyl, C1-4 alkyl or C1-4 alkoxy, A is C1-5 alkylene which may be substituted by hydroxyl, B is carbonyl or methylene which may be substituted by C1-4 alkyl, and R4 and R5 are each C1-4 alkyl, or R4 is hydrogen and R5 is -Z-Ar (wherein Z is C1-5 alkylene, and Ar is aromatic 6-membered ring which may contain nitrogen), or R4 and R5 together form C2-6 cyclic alkylene, or R4 and R5 form together with the adjacent nitrogen atom 4-substituted piperazine of the formula: (see formula II) wherein R6 is C1-4 alkyl). The derivative and its salt are useful as for a vasodilator, an antiallergic drug and an antiplatelet agent.

COMPOUNDS AND METHODS FOR INHIBITION OF HIV AND RELATED VIRUSES

Treatment of Aids, inhibition of the replication of HIV and related viruses, and formulations using thiourea derivative compounds or salts thereof are disclosed. Also disclosed are novel thiourea compounds.

PYRIDAZINONE DERIVATIVES

Pyridazinone derivatives represented by the formula (I) and antiplatelet agents containing them: (see formula I) [wherein R is a hydrogen atom or a C1-C4 alkyl group, X is a hydrogen atom, a chlorine atom or a bromine atom, Ar is a pyridyl group or a phenyl group substituted with OR1 (wherein R1 is a hydrogen atom or a C1-C4 alkyl group) and A {wherein A is a hydrogen atom, a halogen atom, a C1-C4 alkyl group or OR2 (wherein R2 is a hydrogen atom or a C1-C4 alkyl group)}, Y is C1-C8 alkylene wherein one carbon atom on the straight chain is substituted with one OR1 group (wherein R1 is the same as defined above), and Z1 and Z2 are independently a hydrogen atom, a halogen atom, a C1-C4 alkyl group or a OR1 group (wherein R1 is the same as defined above)]. These compounds have strong antiplatelet effects, are excellently safe, and can be used as active ingredients of prophylactic and therapeutic drugs for various thrombotic diseases.

PYRIDAZINONE DERIVATIVES, PROCESSES FOR PRODUCTION THEREOF AND USE THEREOF

Pyridazinone derivatives of formula (I): (I) wherein R1 represents a hydrogen atom or a methyl group which may be substituted with an aliphatic cyclic amino group optionally containing a hetero atom in the ring thereof; each of X1 and X2 independently represents a hydrogen atom, a halogen atom, an alkyl group having 1 to 6 carbon atoms, an alkoxy group having 1 to 6 carbon atoms, a cyano group, a nitro group or a group shown by - CO-NR2R3 (wherein each of R2 and R3 independently represents an alkyl group having 1 to 6 carbon atoms); Y represents a halogen atom; Z represents an alkoxy group having 1 to 6 carbon atoms; ? represents 0 or an integer of 1 to 3; A represents CH or N; m represents 0 or an integer of 1 or 2; and n represents an integer of 1 to 8, exhibit a platelet aggregation inhibiting activity and are useful for the treatment of circulatory disorders such as cerebral infarction.

Verfahren zur Herstellung neuer Pyridazon-(6)-verbindungen

Procédé de préparation de 3-sulfanilamido-pyridazines

Verfahren zur Herstellung neuer Pyridazon-(6)-verbindungen

Verfahren zur Herstellung neuer Tetrahydrodioxopyridazine

Verfahren zur Herstellung acylierter 5-Piperazino-pyridazone-(6)

Verfahren zur Herstellung eines Pyridazons

Verfahren zur Herstellung eines Pyridazons

Verfahren zur Herstellung eines Pyridazons

Verfahren zur Herstellung neuer Halogen-pyridazine

Verfahren zur Herstellung eines Pyridazons.

Verfahren zur Herstellung von 1-Phenyl-4-amino-5-chlorpyridazon-(6)

Procédé pour la préparation de sulfanilamidopyridazines

Verfahren zur Herstellung eines neuen Sulfonamids der Pyridazinreihe

DERIVATIVES OF OXADIAZOLE AND PYRIDAZINE, THEIR PREPARATION AND THEIR APPLICATION IN THERAPEUTICS

The invention relates to compounds of formula (I): 2. The compound of formula (I) as claimed in claim 1 , wherein:W represents a —CH— group;Y represents a —(C3-C10)cycloalkyl-, aryl or aryloxy group, said groups being optionally substituted with one or more substituents chosen from a halogen atom;Z2 is absent; andZ3 is absent or represents a methylene group.3. The compound of formula (I) as claimed in claim 1 , wherein X1 represents a nitrogen atom claim 1 , and X2 and X3 represent a nitrogen atom or an oxygen atom.4. The compound of formula (I) as claimed in claim 1 , wherein X1 represents —CH═CH— claim 1 , and X2 and X3 represent a nitrogen atom.5. The compound of formula (I) as claimed in claim 1 , selected from the group consisting of:trans{4-[4-(5-benzyl[1.2.4]oxadiazol-3-ylcarbamoyl)phenyl]cyclohexyl}acetic acid,trans{4-[4-(3-benzyl[1.2.4]oxadiazol-5-ylcarbamoyl)phenyl]cyclohexyl}acetic acid,cis-4-[4-(3-benzyl[1.2.4]oxadiazol-5-ylcarbamoyl)phenoxy]cyclohexanecarboxylic acid,cis-4-{4-[3-(3,5-difluorobenzyl)[1.2.4]oxadiazol-5-ylcarbamoyl]phenoxy}cyclohexanecarboxylic acid,cis-4-{4-[3-(1-phenylcyclopropyl)[1.2.4]oxadiazol-5-ylcarbamoyl]phenoxy}-cyclohexanecarboxylic acid,cis-4-{4-[3-(1-methyl-1-phenylethyl)[1.2.4]oxadiazol-5-ylcarbamoyl]phenoxy}-cyclohexanecarboxylic acid,cis-4-[4-(3-phenoxymethyl[1.2.4]oxadiazol-5-ylcarbamoyl)phenoxy]cyclohexanecarboxylic acid,{4-[4-(6-benzylpyridazin-3-ylcarbamoyl)phenyl]cyclohexyl}acetic acid,cis-4-[4-(6-cyclopentylaminopyridazin-3-ylcarbamoyl)phenoxy]cyclohexanecarboxylic acid,cis-4-[5-(3-benzyl[1.2.4]oxadiazol-5-ylcarbamoyl)pyridin-2-yloxy]cyclohexanecarboxylic acid,trans-2-{4-[4-(3-benzyl[1.2.4]oxadiazol-5-ylcarbamoyl)phenyl]cyclohexyl}-cyclopropanecarboxylic acid,trans-(E)-3-{4-[4-(3-benzyl[1.2.4]oxadiazol-5-ylcarbamoyl)phenyl]cyclohexyl}-acrylic acid,trans-3-{4-[4-(3-benzyl[1.2.4]oxadiazol-5-ylcarbamoyl)phenyl]cyclohexyl}-propionic acid,cis-4-[4-(6-phenylaminopyridazin-3-ylcarbamoyl)phenoxy]cyclohexanecarboxylic acid, ...

Benzamide derivatives as p2x7 receptor antagonists

The invention relates to benzamide derivatives of formula (I), wherein R 1 , R 2 , R 3 , R 4 , R 5 , R 6 , n and Y are as defined in the description, their preparation and their use as pharmaceutically active compounds.

INTERMEDIATES FOR PREPARING HERBICIDAL PYRIDAZINONES

Disclosed is a compound of Formula I, including N-oxides, and salts thereof, wherein R, Rand Rare defined as set forth in the disclosure. Also disclosed is a process for preparing a compound of Formula I. A compound of Formula I can also be used as a synthetic intermediate to prepare pyridazinone-based herbicides. 3. The compound of wherein{'sup': '1', 'sub': 1', '4, 'Ris C-Calkyl; and'}{'sup': '4', 'Ris methyl, ethyl, n-propyl or i-propyl.'}4. The compound of wherein{'sup': '1', 'Ris methyl; and'}{'sup': '4', 'Ris methyl.'}6. The compound of wherein{'sup': '1', 'sub': 1', '4, 'Ris C-Calkyl; and'}{'sup': '4', 'Ris methyl, ethyl, n-propyl or i-propyl.'}7. The compound of wherein{'sup': '1', 'Ris methyl; and'}{'sup': '4', 'Ris methyl.'}9. The process of wherein Ris methyl.11. The process of wherein Ris methyl.12. The process of wherein Ris methyl. The present disclosure provides pyridazinones and a process for preparing pyridazinones. The pyridazinones disclosed herein can be used as synthetic intermediates to prepare pyridazinone-based herbicides. WO 2015/168010 and WO 2017/074988 disclose herbicidal pyridazinones and synthetic intermediates used to prepare herbicidal pyridazinones. There exists a need for improved methods of preparing herbicidal pyridazinones.In one aspect, the present disclosure provides a compound of Formula I and N-oxides or salts thereof,whereinIn another aspect, the present disclosure provides a process for preparing a compound of Formula I-A,whereinwhereinIn another aspect, the present disclosure provides a process for preparing a compound of Formula I-BwhereinAs used herein, the terms “comprises,” “comprising,” “includes,” “including,” “has,” “having,” “contains”, “containing,” “characterized by” or any other variation thereof, are intended to cover a non-exclusive inclusion, subject to any limitation explicitly indicated. For example, a process or method that comprises a list of elements is not necessarily limited to only those elements but ...

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- ...

BIARYL AMIDE COMPOUNDS AS KINASE INHIBITORS

The present invention provides compounds of Formula (I) as described herein, and salts thereof, and therapeutic uses of these compounds for treatment of disorders associated with Raf kinase activity. The invention further provides pharmaceutical compositions comprising these compounds, and compositions comprising these compounds and a therapeutic co-agent. 120-. (canceled)22. A pharmaceutical composition comprising a compound of or a pharmaceutically acceptable salt thereof and one or more pharmaceutically acceptable carriers.23. A combination comprising a therapeutically effective amount of a compound according to or a pharmaceutically acceptable salt thereof and one or more therapeutically active co-agents.24. A method of treating a proliferative disorder selected from non-small cell lung cancer and ovarian cancer claim 31 , comprising administering to a subject in need thereof a therapeutically effective amount of a compound of or a pharmaceutically acceptable salt thereof.2527-. (canceled) The invention provides compounds that inhibit Raf kinases, and are accordingly useful for treating certain disorders associated with excessive Raf kinase activity, including cell proliferation disorders such as cancers. The invention further provides pharmaceutical compositions containing these compounds and methods of using these compounds to treat conditions including cancer.Protein Kinases are involved in very complex signaling cascades that regulate most cellular functions, including cell survival and proliferation. These signaling pathways have been heavily studied, particularly in the context of disorders caused by dysregulated cellular function, such as cancer. The mitogen-activated protein kinase (MAPK) cascade has been studied extensively, for example, and kinases in this pathway (e.g., RAS, RAF, MEK, and ERK) have been exploited as target sites for drug discovery. Mutated B-Raf is found in a significant fraction of malignancies (over 30% of all tumors and 40% of ...

NOVEL PHENOL DERIVATIVES AND PHARMACEUTICAL OR COSMETIC USE THEREOF

The present invention relates to novel compounds of general formula: 29.-. (canceled) The present invention relates to novel compounds of general formula:and to the cosmetic or pharmaceutical use thereof.The present invention proposes to provide novel phenolic derivatives which are powerful androgen receptor modulators.Among the prior art documents describing molecules which modulate androgen receptor activity, mention may, for example, be made of the phenylimidazolines described in patent application EP 580 459, or application WO 2005/42464.The invention relates to novel phenolic derivatives that correspond to general formula (I) below:in which:The compounds of formula (I) may comprise one or more asymmetric carbon atoms. They may thus exist in the form of a mixture of enantiomers or of diastereoisomers. These enantiomers and diastereoisomers, and also mixtures thereof, including racemic mixtures, form part of the invention.The compounds of formula (I) may exist in the form of bases or of acid-addition salts. Such addition salts form part of the invention. These salts are advantageously prepared with pharmaceutically acceptable acids, but the salts of other acids that are useful, for example for purifying or isolating the compounds of formula (I), also form part of the invention. These acids may be, for example, picric acid, oxalic acid or an optically active acid, for example a tartaric acid, a dibenzoyltartaric acid, a mandelic acid or a camphorsulphonic acid, and those that form physiologically acceptable salts, such as hydrochloride, hydrobromide, sulphate, hydrogen sulphate, dihydrogen phosphate, maleate, fumarate, 2-naphthalenesulphonate or para-toluenesulphonate. For a review of physiologically acceptable salts, see the Handbook of Pharmaceutical Salts: Properties, Selection and Use by Stahl and Wermuth (Wiley-VCH, 2002).The solvates or hydrates may be obtained directly after the synthesis process, compound (I) being isolated in the form of a hydrate, for ...

6-OXO-1,6-DIHYDROPYRIDAZINE DERIVATIVE, PREPARATION METHOD THEREFOR AND MEDICAL USE THEREOF

A 6-oxo-1,6-dihydropyridazine derivative, a preparation method therefor and medical use thereof, in particular, a 6-oxo-1,6-dihydropyridazine derivative represented by general formula (I), a preparation method therefor, and a pharmaceutical composition containing the derivative, and use thereof as a Nav inhibitor and use thereof in the preparation of a drug for the treatment and/or prevention of pain and pain-related diseases. Each substituent in general formula (I) is the same as defined in the description. 3. The compound of formula (I) or the tautomer claim 1 , mesomer claim 1 , racemate claim 1 , enantiomer claim 1 , diastereomer thereof claim 1 , or mixture thereof claim 1 , or the pharmaceutically acceptable salt thereof according to claim 1 , wherein M is selected from the group consisting of O atom claim 1 , CHand S atom.6. The compound of formula (I) or the tautomer claim 1 , mesomer claim 1 , racemate claim 1 , enantiomer claim 1 , diastereomer thereof claim 1 , or mixture thereof claim 1 , or the pharmaceutically acceptable salt thereof according to claim 1 , wherein each Ris identical or different and each is independently selected from the group consisting of hydrogen atom claim 1 , halogen claim 1 , alkyl claim 1 , alkoxy claim 1 , haloalkyl and haloalkoxy.7. The compound of formula (I) or the tautomer claim 1 , mesomer claim 1 , racemate claim 1 , enantiomer claim 1 , diastereomer thereof claim 1 , or mixture thereof claim 1 , or the pharmaceutically acceptable salt thereof according to claim 1 , wherein each Ris identical or different and each is independently selected from the group consisting of hydrogen atom claim 1 , halogen claim 1 , alkyl claim 1 , deuterated alkyl claim 1 , alkoxy claim 1 , deuterated alkoxy claim 1 , hydroxy claim 1 , haloalkyl claim 1 , haloalkoxy claim 1 , cycloalkyl and cycloalkyloxy.8. The compound of formula (I) or the tautomer claim 1 , mesomer claim 1 , racemate claim 1 , enantiomer claim 1 , diastereomer thereof claim ...

THERAPEUTIC COMPOUNDS AND USES THEREOF

The present invention relates to compounds of formula (I): 2. The compound of wherein Ris 2-hydroxy phenyl that is optionally substituted with one or more groups independently selected from the group consisting of halo.34-. (canceled)5. The compound of wherein Ris H claim 1 , methyl claim 1 , or acetyl; and Ris H.6. (canceled)7. The compound of wherein Ris a 3-15 membered heterocyclyl that is optionally substituted with one or more groups independently selected from the group consisting of R claim 1 , oxo claim 1 , halo claim 1 , —NO claim 1 , —N(R) claim 1 , —CN claim 1 , —C(O)—N(W) claim 1 , —S(O)—N(R) claim 1 , —S(O)—N(R) claim 1 , —S—R claim 1 , —O—C(O)—R claim 1 , —C(O)—R claim 1 , —C(O)—R claim 1 , —S(O)—R claim 1 , —S(O)—R claim 1 , —N(R)—C(O)—R claim 1 , —N(R)—S(O)—R claim 1 , —N(R)—C(O)—N(R) claim 1 , and —N(R)—S(O)—R.9. The compound of wherein Ris an N-linked 3-15 membered heterocyclyl that is optionally substituted with one or more groups independently selected from the group consisting of R claim 1 , oxo claim 1 , halo claim 1 , —NO claim 1 , —N(R) claim 1 , —CN claim 1 , —C(O)—N(R) claim 1 , —S(O)—N(R) claim 1 , —S(O)—N(R) claim 1 , —S—R claim 1 , —O—C(O)—R claim 1 , —C(O)—R claim 1 , —C(O)—OR claim 1 , —S(O)—R—S(O)—R claim 1 , —N(R)—C(O)—R claim 1 , —N(R)—S(O)—R claim 1 , —N(R)—C(O)—N(R) claim 1 , and —N(R)—S(O)—R.11. The compound of wherein Ris —O—R.13. The compound of wherein Ris —N(R).15. The compound of wherein Ris selected from the group consisting of —Rand —C(O)—N(R).21. (canceled)23. A composition comprising a compound of formula (I) as described in claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , and a pharmaceutically acceptable adjuvant claim 1 , carrier claim 1 , or vehicle.2425-. (canceled)26. A method for treating a BRG1-mediated disorder claim 1 , a BRM-mediated disorder and/or a PB1-mediated disorder in an animal comprising administering a compound of formula (I) as described in claim 1 , or a pharmaceutically acceptable ...

N-(HETEROARYL)-SULFONAMIDE DERIVATIVES USEFUL AS S100-INHIBITORS

A compound of formula (I), or a pharmaceutically acceptable salt thereof and a pharmaceutical composition comprising the compound. The compound is an inhibitor of interactions between S100A9 and interaction partners such as RAGE, TLR4 and EMMPRIN and as such is useful in the treatment of disorders such as cancer, autoimmune disorders, inflammatory disorders and neurodegenerative disorders. 2. The compound of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein Ris H or halogen and Ris halogen or cyano.3. The compound of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein Ris H or halogen claim 1 , and Ris H claim 1 , C1-C3 alkyl optionally substituted with one or more F; or C1-C3 alkoxy optionally substituted with one or more F.4. The compound of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein Rand Rare halogens.8. The compound of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein Y is CR.9. The compound of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein W is N.10. (canceled)11. The compound of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein X is N.12. The compound of claim 9 , or a pharmaceutically acceptable salt thereof claim 9 , wherein W and X are N.13. (canceled)14. The compound of claim 11 , or a pharmaceutically acceptable salt thereof claim 11 , wherein Y is CH claim 11 , Z is CR claim 11 , and Ris halogen.15. The compound of claim 12 , or a pharmaceutically acceptable salt thereof claim 12 , wherein Y is CR claim 12 , Z is CH claim 12 , and Ris halogen or S(O)C1-C3 alkyl.16. (canceled)17. (canceled)18. (canceled)19. The compound of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein m is 1 and Ris H.20. The compound of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein m is 0.22. (canceled)23. A pharmaceutical composition comprising a compound according to claim 1 , or a ...

SUBSTITUTED CARBONUCLEOSIDE DERIVATIVES USEFUL AS ANTICANCER AGENTS

Compounds of the general formula): 125-. (canceled)28. The method of claim 27 , wherein the cancer is lung cancer claim 27 , bone cancer claim 27 , pancreatic cancer claim 27 , skin cancer claim 27 , cancer of the head or neck claim 27 , cutaneous or intraocular melanoma claim 27 , uterine cancer claim 27 , ovarian cancer claim 27 , rectal cancer claim 27 , cancer of the anal region claim 27 , stomach cancer claim 27 , colon cancer claim 27 , breast cancer claim 27 , uterine cancer claim 27 , carcinoma of the fallopian tubes claim 27 , carcinoma of the endometrium claim 27 , carcinoma of the cervix claim 27 , carcinoma of the vagina claim 27 , carcinoma of the vulva claim 27 , Hodgkin's Disease claim 27 , cancer of the esophagus claim 27 , cancer of the small intestine claim 27 , cancer of the endocrine system claim 27 , cancer of the thyroid gland claim 27 , cancer of the parathyroid gland claim 27 , cancer of the adrenal gland claim 27 , sarcoma of soft tissue claim 27 , cancer of the urethra claim 27 , cancer of the penis claim 27 , prostate cancer claim 27 , chronic or acute leukemia claim 27 , lymphocytic lymphomas claim 27 , cancer of the bladder claim 27 , cancer of the kidney or ureter claim 27 , renal cell carcinoma claim 27 , carcinoma of the renal pelvis claim 27 , neoplasms of the central nervous system (CNS) claim 27 , primary CNS lymphoma claim 27 , spinal axis tumors claim 27 , brain stem glioma claim 27 , or pituitary adenoma.29. The method of claim 27 , wherein the cancer is lymphoma.30. The method of claim 27 , wherein the cancer is colon cancer.31. The method of claim 27 , wherein the cancer is esophageal cancer.32. The method of claim 27 , wherein the cancer is stomach cancer.33. The method of claim 27 , wherein the cancer is lung cancer.34. The method of claim 27 , wherein the cancer is breast cancer.35. The method of claim 27 , wherein the cancer is ovarian cancer.36. The method of claim 27 , wherein the cancer is bladder cancer.37. The method ...

Novel Heterocyclic Compounds as Bromodomain Inhibitors

The present disclosure relates to compounds, which are useful for inhibition of BET protein function by binding to bromodomains, and their use in therapy.

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.

HETEROCYCLIC COMPOUNDS AS BET INHIBITORS

Novel bromodomain and extraterminal domain (BET) inhibitors and to therapeutic methods of treating conditions and diseases using these novel BET inhibitors are provided. 6. The compound of claim 1 , or a tautomer or isomer thereof claim 1 , or a pharmaceutically acceptable salt of any of the foregoing claim 1 , wherein X is O.7. The compound of claim 1 , or a tautomer or isomer thereof claim 1 , or a pharmaceutically acceptable salt of any of the foregoing claim 1 , wherein Ris hydrogen claim 1 , C-Calkyl optionally substituted by —OH claim 1 , C-Ccycloalkyl optionally substituted by C-Calkyl claim 1 , C-Chaloalkyl claim 1 , C-Calkoxy claim 1 , —CN claim 1 , —(CH)N(R)WR claim 1 , or —(CH)WR.8. The compound of claim 1 , or a tautomer or isomer thereof claim 1 , or a pharmaceutically acceptable salt of any of the foregoing claim 1 , wherein Ris C-Calkyl optionally substituted by —OH.9. The compound of claim 1 , or a tautomer or isomer thereof claim 1 , or a pharmaceutically acceptable salt of any of the foregoing claim 1 , wherein Ris hydrogen claim 1 , —(CH)N(R)WR claim 1 , or —(CH)WR.10. The compound of claim 1 , or a tautomer or isomer thereof claim 1 , or a pharmaceutically acceptable salt of any of the foregoing claim 1 , wherein Ris hydrogen claim 1 , —NRC(O)R claim 1 , —NRS(O)R claim 1 , NRC(O)NRR claim 1 , —NRS(O)NRR claim 1 , —(CH)N(R)WR claim 1 , —(CH)WR claim 1 , or C-Calkyl optionally substituted by halogen claim 1 , oxo claim 1 , —CN or —OH.11. The compound of claim 1 , or a tautomer or isomer thereof claim 1 , or a pharmaceutically acceptable salt of any of the foregoing claim 1 , wherein Gis N.12. The compound of claim 1 , or a tautomer or isomer thereof claim 1 , or a pharmaceutically acceptable salt of any of the foregoing claim 1 , wherein Gis CR claim 1 , wherein Ris hydrogen.13. The compound of claim 1 , or a tautomer or isomer thereof claim 1 , or a pharmaceutically acceptable salt of any of the foregoing claim 1 , wherein Gis N.14. The compound ...

N-(HETEROARYL)-SULFONAMIDE DERIVATIVES USEFUL AS S100-INHIBITORS

A compound of formula (I), or a pharmaceutically acceptable salt thereof and a pharmaceutical composition comprising the compound. The compound is an inhibitor of interactions between SI 00A9 and interaction partners such as RAGE, TLR4 and EMMPRIN and as such is useful in the treatment of disorders such as cancer, autoimmune disorders, inflammatory disorders and neurodegenerative disorders. 5. The method of claim 1 , wherein one of Rand Ris halogen and the other one is selected from H claim 1 , halogen claim 1 , cyano claim 1 , C1-C3 alkyl optionally substituted with one or more F; C1-C3 alkylthio optionally substituted with one or more F; C1-C3 alkoxy optionally substituted with one or more F; and C(O)NRR.6. The method of claim 1 , wherein Ris H or halogen and Ris halogen or cyano.7. The method of claim 1 , wherein Ris H or halogen claim 1 , and Ris H claim 1 , C1-C3 alkyl optionally substituted with one or more F; or C1-C3 alkoxy optionally substituted with one or more F.8. The method of claim 1 , wherein Rand Rare halogens.9. The method of claim 1 , wherein Y is CR.10. The method of claim 1 , wherein W is N.11. The method of claim 1 , wherein X is N.12. The method of claim 1 , wherein Y is CH claim 1 , Z is CR claim 1 , and Ris halogen.13. The method of claim 1 , wherein Y is CR claim 1 , Z is CH claim 1 , and Ris halogen or S(O)C1-C3 alkyl.14. The method of claim 1 , wherein m is 1 and Ris H.15. The method of claim 1 , wherein m is 0.16. The method of claim 1 , wherein the compound is selected from5-bromo-6-chloro-N-(5-chloro-2-hydroxypyridin-3-yl)pyridine-3-sulfonamide;N-(4-hydroxypyridin-3-yl)benzenesulfonamide;N-(4-hydroxypyridin-3-yl)-4-(trifluoromethyl)benzene-1-sulfonamide;N-(4-hydroxypyridin-3-yl)-4-(trifluoromethoxy)benzene-1-sulfonamide;N-(5-chloro-3-hydroxypyridin-2-yl)-1-phenylmethanesulfonamide;N-(5-chloro-3-hydroxypyridin-2-yl)-6-(pyrrolidin-1-yl)pyridine-3-sulfonamide;N-(5-chloro-3-hydroxypyridin-2-yl)pyridine-3-sulfonamide;6-chloro-N-(5-chloro-3- ...

BIARYL AMIDE COMPOUNDS AS KINASE INHIBITORS

The present invention provides compounds of Formula (I) 2. The method of wherein the proliferative disease is a cancer selected from solid tumors claim 1 , melanoma claim 1 , breast cancer claim 1 , non-small cell lung cancer claim 1 , lung adenocarcinoma claim 1 , sarcoma claim 1 , gastrointestinal stromal tumors claim 1 , ovarian cancer claim 1 , colorectal cancer claim 1 , thyroid cancer and pancreatic cancer.3. The method of wherein the proliferative disease is melanoma.5. The method of wherein the proliferative disease is a cancer selected from solid tumors claim 4 , melanoma claim 4 , breast cancer claim 4 , non-small cell lung cancer claim 4 , lung adenocarcinoma claim 4 , sarcoma claim 4 , gastrointestinal stromal tumors claim 4 , ovarian cancer claim 4 , colorectal cancer claim 4 , thyroid cancer and pancreatic cancer.6. The method of wherein the proliferative disease is melanoma.8. The method of wherein the one or more therapeutically active co-agents is a RAF pathway inhibitor selected from paclitaxel claim 7 , docetaxel claim 7 , temozolomide claim 7 , platins claim 7 , doxorubicins claim 7 , vinblastins claim 7 , cyclophosphamide claim 7 , topotecan claim 7 , gemcitabine claim 7 , ifosfamide claim 7 , etoposide and irinotecan.9. The method of wherein the proliferative disease is a cancer selected from solid tumors claim 8 , melanoma claim 8 , breast cancer claim 8 , non-small cell lung cancer claim 8 , lung adenocarcinoma claim 8 , sarcoma claim 8 , gastrointestinal stromal tumors claim 8 , ovarian cancer claim 8 , colorectal cancer claim 8 , thyroid cancer and pancreatic cancer.10. The method of wherein the proliferative disease is melanoma. This application is a Divisional of U.S. patent application Ser. No. 15/601,423, filed on May 22, 2017, which is a Divisional of U.S. patent application Ser. No. 14/774,431, filed on Sep. 10, 2015, now U.S. Pat. No. 9,694,016, which is a 371 of international application PCT/US2014/026107, filed on Mar. 13, 2014, ...

BIARYL AMIDE COMPOUNDS AS KINASE INHIBITORS

The present invention provides compounds of Formula (I) as described herein, and salts thereof, and therapeutic uses of these compounds for treatment of disorders associated with Raf kinase activity. The invention further provides pharmaceutical compositions comprising these compounds, and compositions comprising these compounds and a therapeutic co-agent. 131-. (canceled)331. A pharmaceutical composition comprising a compound of claim or a pharmaceutically acceptable salt thereof and one or more pharmaceutically acceptable carriers.341. A combination comprising a therapeutically effective amount of a compound according to claim or a pharmaceutically acceptable salt thereof and one or more therapeutically active co-agents.351. A method of treating a proliferative disorder selected from non-small cell lung cancer and ovarian cancer , comprising administering to a subject in need thereof a therapeutically effective amount of a compound of claim or a pharmaceutically acceptable salt thereof. The invention provides compounds that inhibit Raf kinases, and are accordingly useful for treating certain disorders associated with excessive Raf kinase activity, including cell proliferation disorders such as cancers. The invention further provides pharmaceutical compositions containing these compounds and methods of using these compounds to treat conditions including cancer.Protein Kinases are involved in very complex signaling cascades that regulate most cellular functions, including cell survival and proliferation. These signaling pathways have been heavily studied, particularly in the context of disorders caused by dysregulated cellular function, such as cancer. The mitogen-activated protein kinase (MAPK) cascade has been studied extensively, for example, and kinases in this pathway (e.g., RAS, RAF, MEK, and ERK) have been exploited as target sites for drug discovery. Mutated B-Raf is found in a significant fraction of malignancies (over 30% of all tumors and 40% of melanomas ...

Cannabinoid-2 agonists

The present specification discloses cannabinoid-2 agonists, compositions comprising such cannabinoid-2 agonists, and methods of treating an individual suffering from a disease by administering compositions comprising such cannabinoid-2 agonists.

CYCLOHEXYL SULFONE ROR GAMMA MODULATORS

Described are RORγ modulators of the formula (I), or stereoisomers, tautomers, pharmaceutically acceptable salts, solvates, or prodrugs thereof, wherein all substituents are defined herein. Also provided are pharmaceutical compositions comprising the same. Such compounds and compositions are useful in methods for modulating RORγ activity in a cell and methods for treating a subject suffering from a disease or disorder in which the subject would therapeutically benefit from modulation of RORγ activity, for example, autoimmune and/or inflammatory disorders. 2. A compound according to claim 1 , or a stereoisomer or pharmaceutically-acceptable salt thereof claim 1 , wherein Ris CF.3. A compound according to claim 1 , or a stereoisomer or pharmaceutically-acceptable salt thereof claim 1 , wherein{'sup': 1', '1a', '1a, 'sub': '1-6', 'Ris halo, phenyl substituted with 0-3 R, or Calkyl substituted with 0-3 R; and'}{'sup': 1a', 'a', 'b', 'f, 'sub': 3', '1-6', '2', 'r', '2', 'r, 'Ris, independently at each occurrence, hydrogen, CF, halo, Calkyl substituted with 0-3 R, —(CH)OR, and —(CH)-phenyl substituted with 0-3 R.'}4. A compound according to claim 1 , or a stereoisomer or pharmaceutically-acceptable salt thereof claim 1 , wherein:{'sup': 2', '2b', '2b', '2b', '11', '11', '2b', '2c', '2b', '2c', '11', '11', '2b', '11', '11', '2b', 'c', '2a', '2', '2', '2a', '2a, 'sub': 2', 'r', '2', 'r', '2', 'r', '2', 'r', '2', 'r', '2', 'r', '2', 'r', '2', 'r', 'p', '1-6', '2', 'r', 'p', 'p, 'Ris, independently at each occurrence, selected from hydrogen, ═O, —(CH)OR, —(CH)C(O)R, —(CH)OC(O)OR, —(CH)OC(O)NRR, —(CH)NRC(O)R, —(CH)NRC(O)OR, —(CH)NRR, —(CH)NRC(O)NRR, —NRS(O)R, Calkyl, —(CH)-4-10 membered heterocycle comprising carbon atoms, and 1-4 heteroatoms selected from N, O, and S(O)substituted with 0-3 R; or one Rtogether with an Ron an adjacent carbon combine to form a fused ring substituted with 0-3 R, wherein the fused ring is selected from a 4-7 membered heterocycle comprising carbon ...

SUBSTITUTED CARBONUCLEOSIDE DERIVATIVES USEFUL AS ANTICANCER AGENTS

Compounds of the general formula): 12. A compound of any of - , wherein said salt is selected from acetate , aspartate , benzoate , besylate , bicarbonate/carbonate , bisulphate/sulfate , borate , camsylate , citrate , edisylate , esylate , formate , fumarate , gluceptate , gluconate , glucuronate , hexafluorophosphate , hibenzate , hydrochloride/chloride , hydrobromide/bromide , hydroiodide/iodide , isethionate , lactate , malate , maleate , malonate , mesylate , methylsulfate , naphthylate , 2-napsylate , nicotinate , nitrate , orotate , oxalate , palmitate , pamoate , phosphate/hydrogen phosphate/dihydrogen phosphate , saccharate , stearate , succinate , tartrate , tosylate , trifluoroacetate , aluminum , arginine , benzathine , calcium , choline , diethylamine , diolamine , glycine , lysine , magnesium , meglumine , olamine , potassium , sodium , tromethamine and zinc salts.13. A compound of any of - , wherein said salt is selected from hydrochloride , tosylate and mesolate salts.14. A pharmaceutical composition comprising a compound according to any one of - or a pharmaceutically acceptable salt thereof , and a pharmaceutically acceptable carrier.15. A method of treating abnormal cell growth in a mammal , the method comprising administering to the mammal a therapeutically effective amount of a compound according to any one of - or a pharmaceutically acceptable salt thereof.16. The method of claim 15 , wherein the abnormal cell growth is cancer.17. The method of claim 16 , wherein the cancer is lung cancer claim 16 , bone cancer claim 16 , pancreatic cancer claim 16 , skin cancer claim 16 , cancer of the head or neck claim 16 , cutaneous or intraocular melanoma claim 16 , uterine cancer claim 16 , ovarian cancer claim 16 , rectal cancer claim 16 , cancer of the anal region claim 16 , stomach cancer claim 16 , colon cancer claim 16 , breast cancer claim 16 , uterine cancer claim 16 , carcinoma of the fallopian tubes claim 16 , carcinoma of the endometrium claim ...

Inhibitors of Dihydroceramide Desaturase For Treating Disease

Disclosed herein are dihydroceramide desaturase 1 (Des1) inhibitor compounds and compositions, which are useful in the treatment of diseases, such as metabolic disorders, where inhibition of Des1 is expected to be therapeutic to a patient. Methods of inhibition of Des1 activity in a human or animal subject are also provided.

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 lower alkoxyl group, a lower alkylthio group or a halogen atom; R 2 represents H, a lower alkoxyl group, a lower alkylthio group or a halogen atom; R 3 represents a lower alkyl or lower alkenyl group, which may be substituted by one or more OHs, CNs, lower cycloalkyl groups, (substituted) aromatic groups or (substituted) carbamoyl groups; R 4 represents COOH, a lower alkoxycarbonyl group, a (substituted) carbamoyl group, a (substituted) amino group, or a (substituted) ureido group; 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.

Pyridazinone derivatives and use thereof as p2x7 receptor inhibitors

Novel pyridazinone compounds of formula (I), which inhibit the purinergic P2X7 receptor and are useful for prevention, therapy and improvement of inflammatory and immunological diseases.

Method of producing derivatives of dihydropyridazinone

Compounds of the formula (I): …<CHEM>… and pharmaceutically acceptable salts are described, wherein R<1> is hydrogon or methyl and R<2> is hydrogen or C1-4alkyl. These compounds have inotropic, vasodilator, bronchodilating and platelet aggregation inhibiting properties. Pharmaceutical compositions are described as are methods of use. Intermediates and processes for the preparation of the compounds of the formula (I) are described.

Process for producing pyridazinylhydrazones or their acid additive salts

Pyridazinylhydrazones capable of lowering blood pressure having the formula <IMAGE> wherein R1 is hydrogen, chlorine, alkyl having from 1 to 4 carbon atoms, methoxy, hydroxyl, carbamoyl or cyano; R2 is morpholino; and K is a group having the formula <IMAGE> wherein one of R3, R4, R5 or R6 is carboxyl or alkoxycarbonyl.

4-aminophenol derivatives or their n-alkyl or salt derivatives showing antiinflammatory activity

FIELD: organic chemistry. SUBSTANCE: product: derivatives of 4-aminophenol of the formula (I) where R 1 group -C(O)YZ where Y a simple bond, O, -NR 7 or CO; Z H, pyridyl, phenyl that can be substituted for halogen, nitro, lower alkoxy or carboxy; lower alkyl which can be substituted for -OH, lower alkoxy, lower acyloxy, carboxy, lower alkoxycarbonyl, CONR 8 , phenyl(lower)alkoxy, phenyl, halide, cyano or NR 10 R 12 ; R 2 , R 3 , R 6 anf R 5 H, lower alkyl or alkenyl, lower alkoxy or halogen; R 4 and R 7 H or lower alkyl; X 4,5-dihydropyrazolyl or pyrazolyl which can be substituted for C 3 -C 6 -cycloalkyl or phenyl which can be substituted for trihaloidalkyl; R 8 , R 9 , R 10 and R 11 H, lower alkyl or benzylhydroxycarbonyl, or their N-acyl or salt derivatives. Synthesized compounds were used in medicine. EFFECT: improved method of synthesis. 6 cl 611670сС ПЧ Го РОССИЙСКОЕ АГЕНТСТВО ПО ПАТЕНТАМ И ТОВАРНЫМ ЗНАКАМ (19) ВИ "” 2049 779‘ (51) МПК 13) СЛ 31/415 С 070 231/38, 401/12, А 61 К 12) ОПИСАНИЕ ИЗОБРЕТЕНИЯ К ПАТЕНТУ РОССИЙСКОЙ ФЕДЕРАЦИИ (21), (22) Заявка: 4894663/04, 17.05.1990 (30) Приоритет: 20.05.1989 СВ 8911654.5 20.05.1989 СВ 8911655.2 10.02.1990 СВ 9003044.6 (46) Дата публикации: 10.12.1995 (56) Ссылки: Майтаа!е; ТПе ехга рпагтасорета, 291 еЧШоп, ед. |атез Е.ЁГ.Кеупо!|С$, Гопаоп, ТПе Рвагтасеийса! Ргез$$, 1989, р.1584.А.Наскват К./. СиЯ\А$, С.НаНат, /.Мапп, Р.О. Мигпей, А.А. Моггзо| М\.Т. Зитрзоп, Адет5$ апа АсНопз, 30, 432.ЕР М 0254259, кл. С 07О 241/20, опублик. 1988. (86) Заявка РСТ: РСТ/СВ 90/00762 (17.05.90) (71) Заявитель: Физонз ПЛС (СВ) (72) Изобретатель: Джон Раймонд Бантик[СВ], Дэвид Норман Хардерн[ГСВ], Ричард Энтони Эпплтон[ СВ], Джон Диксон[ СВ], Дэвид Джон Уилкинсон[ СВ] (73) Патентообладатель: Физонз ПЛС (СВ) (54) ПРОИЗВОДНЫЕ 4-АМИНОФЕНОЛА ИЛИ ИХ М-АЛКИЛЬНЫЕ ИЛИ СОЛЕВЫЕ ПРОИЗВОДНЫЕ, ПРОЯВЛЯЮЩИЕ ПРОТИВОВОСПАЛИТЕЛЬНУЮ АКТИВНОСТЬ (57) Реферат: Использование: в медицине в качестве веществ, обладающих противовоспалительной активностью. Сущность ...

Производные пиридазинона и ингибиторы р2х7 рецептора

1. Соединение, представленное формулой (I) ! ! где R1 означает атом водорода, гидроксигруппу, нитрогруппу, цианогруппу, карбоксигруппу, карбамоильную группу, аминогруппу, атом галогена, C1-6алкильную группу, C2-6алкенильную группу, C2-6алкинильную группу или C1-6алкоксигруппу (C1-6алкильная группа, C2-6алкенильная группа, C2-6алкинильная группа и C1-6алкоксигруппа являются незамещенными или замещены одним или несколькими атомами галогена), ! R2 означает атом водорода, гидроксигруппу, нитрогруппу, цианогруппу, карбоксигруппу, карбамоильную группу, аминогруппу, атом галогена, C1-6алкильную группу, C2-6алкенильную группу, C1-6алкоксигруппу, моно-C1-6алкиламиногруппу, ди-C1-6алкиламиногруппу, C1-6алкилтиогруппу или C1-6алкилсульфонильную группу (C1-6алкильная группа, C2-6алкенильная группа, C1-6алкоксигруппа, моно-C1-6алкиламиногруппа, ди-C1-6алкиламиногруппа, C1-6алкилтиогруппа и C1-6алкилсульфонильная группа являются незамещенными или замещены одним или несколькими атомами галогена), ! Q означает любую из структур, представленных формулами (II) ! ! (где каждый из R3 и R5 независимо означает атом водорода, C1-6алкильную группу, C2-6алкенильную группу или C2-6алкинильную группу (C1-6алкильная группа, C2-6алкенильная группа и C2-6алкинильная группа являются незамещенными или замещены одним или несколькими атомами галогена), ! R4 означает C1-20алкильную группу, C2-20алкенильную группу или C2-19гетероциклильную группу (C1-20алкильная группа, C2-20алкенильная группа и C2-19гетероциклильная группа являются незамещенными или замещены одним или несколькими одинаковыми или различными заместителями, выбранными из группы V1 заместителей), или ! R3 и R4 означают вместе друг с другом РОССИЙСКАЯ ФЕДЕРАЦИЯ (19) RU (11) 2010 121 763 (13) A (51) МПК C07D 237/20 (2006.01) ФЕДЕРАЛЬНАЯ СЛУЖБА ПО ИНТЕЛЛЕКТУАЛЬНОЙ СОБСТВЕННОСТИ (12) ЗАЯВКА НА ИЗОБРЕТЕНИЕ (21)(22) Заявка: 2010121763/04, 30.10.2008 (71) Заявитель(и): НИССАН КЕМИКАЛ ИНДАСТРИЗ, ЛТД. (JP) Приоритет(ы): (30) Конвенционный ...

Process for producing 4-amino-5-chloro-1-phenylpyrid-azone-(6)

Benzylpyridazinones as inhibitors of reverse transcriptase

Настоящее изобретение относится к соединениям, применимым для лечения заболеваний, опосредуемых вирусом ВИЧ, формулы I где X 1 выбран из R 5 O, R 5 S(O) n , R 5 CH 2 , R 5 CH 2 O, R 5 CH 2 S(O) n , R 5 OCH 2 и R 5 S(O) n CH 2 ; R 1 и R 2 выбраны из Н, NH 2 , алкила, галогеналкила, циклоалкила, алкокси, алкилтио, галогена, алкиламино, диалкиламино, нитро и циано; или совместно образуют -СН=СН-СН=СН- или 5-членный гетероцикл с гетероатомом, выбранным из О и S; R 3 выбран из Н, галогена, нитро и циано; R 4 выбран из Н, NH 2 , алкила, галогеналкила, циклоалкила, алкокси, алкилтио, галогена, алкиламино, диалкиламино, аминоацила, нитро и циано; R 5 выбран из алкила, циклоалкила и необязательно замещенных фенила, нафтила, пиридинила, пиридин-N-оксида, индола, хинолина, хинолин-N-оксида; R 7 и R 8 выбраны из Н, NH 2 , алкиламина, диалкиламина и необязательно замещенного C 1 -С 6 алкила; n выбран из 0, 1, 2. Технический результат - получение новых ингибиторов обратной транскриптазы. 2 н.п. ф-лы, 3 табл.

MEDICINAL PRODUCTS FOR HIV REVERSE TRANSCRIPTASE INHIBITORS

РОССИЙСКАЯ ФЕДЕРАЦИЯ (19) RU (11) (13) 2016 142 611 A (51) МПК A61K 31/501 (2006.01) ФЕДЕРАЛЬНАЯ СЛУЖБА ПО ИНТЕЛЛЕКТУАЛЬНОЙ СОБСТВЕННОСТИ (12) ЗАЯВКА НА ИЗОБРЕТЕНИЕ (21)(22) Заявка: 2016142611, 27.03.2015 (71) Заявитель(и): МЕРК ШАРП И ДОУМ КОРП. (US) Приоритет(ы): (30) Конвенционный приоритет: 01.04.2014 US 61/973,689 (85) Дата начала рассмотрения заявки PCT на национальной фазе: 01.11.2016 R U (43) Дата публикации заявки: 03.05.2018 Бюл. № 13 (72) Автор(ы): БЕРГИ Кристофер С. (US), ФРИЦЕН Джеффри Ф. (US), БАЛСЕЛЛС Хауме (US), ПАТЕЛ Мехул (US) (86) Заявка PCT: (87) Публикация заявки PCT: WO 2015/153304 (08.10.2015) A Адрес для переписки: 129090, Москва, ул. Б.Спасская, 25, строение 3, ООО "Юридическая фирма Городисский и Партнеры" (57) Формула изобретения 1. Соединение структурной формулы I или его фармацевтически приемлемая соль: R U A 2 0 1 6 1 4 2 6 1 1 (54) ПРОЛЕКАРСТВЕННЫЕ СРЕДСТВА ИНГИБИТОРОВ ОБРАТНОЙ ТРАНСКРИПТАЗЫ ВИЧ 2 0 1 6 1 4 2 6 1 1 US 2015/022868 (27.03.2015) Стр.: 1 R U A 2 0 1 6 1 4 2 6 1 1 R2представляет собой галоген или -C1-3-алкил, замещенный 1-3 -F; R3представляет собой (a) галоген, (b) -C1-3-алкил, замещенный 1-3 -F, или (3) фенил, замещенный галогеном; и R4представляет собой . 2. Соединение по п. 1 или его фармацевтически приемлемая соль, где R1представляет собой R U ; . 3. Соединение по п. 1 или его фармацевтически приемлемая соль, Стр.: 2 A где R1представляет собой 2 0 1 6 1 4 2 6 1 1 I, где R1представляет собой . 4. Соединение по любому из пп. 1-3 или его фармацевтически приемлемая соль, где R2представляет собой метил, замещенный 1, 2 или 3 -F; или этил, замещенный 1, 2 или 3 -F. 5. Соединение по п. 4 или его фармацевтически приемлемая соль, где R2представляет собой -CHF2, -CF3 или -CF2CH3. 6. Соединение по любому из пп. 1-5 или его фармацевтически приемлемая соль, где R3представляет собой -F; -Cl; метил, замещенный 1, 2 или 3 -F; этил, замещенный 1, 2 или 3 -F; или фенил, замещенный -F. 7. Соединение по п. 6 или его фармацевтически ...

SUBSTITUTED 6- (1-PIPERAZINYL) -PYRIDAZINES AS 5-HT6 RECEPTOR ANTAGONISTS

1. Соединение формулы (I) !! или его стереоизомерная форма, в которой ! R1 является хлором, трифторметилом или циано; ! R2 является фенилом или фенилом, замещенным галогеном; ! R3 является водородом, С1-4-алкилом или пиридинилметилом; ! X представляет собой -O-, -NH-, -CH2-, -CH(OH)-, -SO2-, -CO-, -NH-CH2-, -О-CH2-, 1,2-этендиил или этиндиил; ! или его фармацевтически приемлемая аддитивная соль или сольват. ! 2. Соединение по п.1, в котором ! R1 является трифторметилом; ! R2 является фенилом или фенилом, замещенным фтором; ! R3 является водородом, метилом или пиридинилметилом; ! X представляет собой -O-, -NH-, -CH2-, -CH(OH)-, -SO2-, -CO-, -NH-CH2-, -О-CH2-, 1,2-этендиил или этиндиил; ! или его фармацевтически приемлемая аддитивная соль или сольват. ! 3. Соединение по п.1, в котором ! R2 является фенилом или фенилом, замещенным фтором. ! 4. Соединение по п.1, в котором соединение представляет собой N-(4-фторфенил)-6-(1-пиперазинил)-3-(трифторметил)-4-пиридазинамин. ! 5. Соединение по п.1, в котором соединение представляет собой N-(4-фторфенил)-6-(1-пиперазинил)-3-(трифторметил)-4-пиридазинамин*2,5 HCl*0,5 H2O. ! 6. Соединение по любому из пп.1-5 для применения в качестве лекарственного средства. ! 7. Соединение по п.6 для применения в качестве лекарственного средства для лечения или предотвращения состояний, в которых поражена когнитивная деятельность; болезни Альцгеймера, болезни Паркинсона, шизофрении, болезни Хантингтона, болезни диффузных телец Леви, слабоумия, вызванного вирусом иммунодефицита человека, слабоумия, вызванного болезнью Крейцфельда-Якоба; амнестических нарушений; умеренных когнитивных нарушений; и возрастного когнитивного отклонения; для лечения и/или предотвращения пищевых нарушений или з (19) РОССИЙСКАЯ ФЕДЕРАЦИЯ RU (11) 2011 103 759 (13) A (51) МПК C07D 237/00 (2006.01) ФЕДЕРАЛЬНАЯ СЛУЖБА ПО ИНТЕЛЛЕКТУАЛЬНОЙ СОБСТВЕННОСТИ (12) ЗАЯВКА НА ИЗОБРЕТЕНИЕ (71) Заявитель(и): ЯНССЕН ФАРМАЦЕВТИКА НВ (BE) (21)(22) Заявка: 2011103759/04, 01.07.2009 ...

Heterocyclic compounds as bromodomain inhibitors

The present disclosure relates to compounds, which are useful for inhibition of BET protein function by binding to bromodomains, and their use in therapy.

Heterocyclic compounds and medicinal use thereof

本发明提供右式表示的杂环化合物,该化合物对于AP－1活性、NF－kappaB活性、炎症性细胞因子生成、基质金属蛋白酶生成、或炎症性细胞粘着因子表达等具有抑制作用,并可用于医药。式中,R 1 表示环烷基、环烯基,R 2 、R 3 表示氢原子或烷基,R 4 表示烷基、环状基团等,n是0～6的整数,A表示杂环,B表示芳香环或杂环,X、Y表示键或连接基团。

Pyridazine derivatives and their use as therapeutic agents

ÐÎÑÑÈÉÑÊÀß ÔÅÄÅÐÀÖÈß RU (19) (11) 2006 105 716 (13) A (51) ÌÏÊ C07D 237/20 (2006.01) ÔÅÄÅÐÀËÜÍÀß ÑËÓÆÁÀ ÏÎ ÈÍÒÅËËÅÊÒÓÀËÜÍÎÉ ÑÎÁÑÒÂÅÍÍÎÑÒÈ, ÏÀÒÅÍÒÀÌ È ÒÎÂÀÐÍÛÌ ÇÍÀÊÀÌ (12) ÇÀßÂÊÀ ÍÀ ÈÇÎÁÐÅÒÅÍÈÅ (21), (22) Çà âêà: 2006105716/04, 29.07.2004 (71) Çà âèòåëü(è): ÇÈÍÎÍ ÔÀÐÌÀÑÜÞÒÈÊËÇ ÈÍÊ. (CA) (30) Êîíâåíöèîííûé ïðèîðèòåò: 30.07.2003 US 60/491,116 30.07.2003 US 60/491,095 (85) Äàòà ïåðåâîäà çà âêè PCT íà íàöèîíàëüíóþ ôàçó: 28.02.2006 (87) Ïóáëèêàöè PCT: WO 2005/011653 (10.02.2005) Àäðåñ äë ïåðåïèñêè: 101000, Ìîñêâà, Ì.Çëàòîóñòèíñêèé ïåð., ä.10, êâ.15, "ÅÂÐÎÌÀÐÊÏÀÒ", È.À.Âåñåëèöêîé R U ÑÐÅÄÑÒ (57) Ôîðìóëà èçîáðåòåíè 1. Ñïîñîá èíãèáèðîâàíè àêòèâíîñòè ñòåàðîèë-ÑîÀ äåñàòóðàçû ÷åëîâåêà (hSCD), âêëþ÷àþùèé êîíòàêòèðîâàíèå èñòî÷íèêà hSCD ñ ñîåäèíåíèåì ôîðìóëû A 2 0 0 6 1 0 5 7 1 6 A (54) ÏÐÎÈÇÂÎÄÍÛÅ ÏÈÐÈÄÀÇÈÍÀ È ÈÕ ÏÐÈÌÅÍÅÍÈÅ Â ÊÀ×ÅÑÒÂÅ ÒÅÐÀÏÅÂÒÈ×ÅÑÊÈÕ ãäå õ è ó êàæäûé íåçàâèñèìî îçíà÷àåò 1, 2 èëè 3; W ïðåäñòàâë åò ñîáîé -Î-, -Ñ(O)O-, -N(R 1)-, -S(O)t (ãäå t îçíà÷àåò 0, 1 èëè 2), -N(R 1)S(O)2-, -ÎÑ(O)- èëè -Ñ(O)-; V ïðåäñòàâë åò ñîáîé -Ñ(O)-, -C(S)-, -C(O)N(R 1)-, -C(O)O-, -S(O)2-, -S(O)2N(R 1)èëè -C(R 11)H-; êàæäûé R 1 íåçàâèñèìî âûáèðàþò èç ãðóïïû, ñîñòî ùåé èç âîäîðîäà, Ñ1-Ñ12àëêèëà, Ñ2-Ñ12ãèäðîêñèàëêèëà, Ñ4-Ñ12öèêëîàëêèëàëêèëà è Ñ7-Ñ19àðàëêèëà; R 2 âûáèðàþò èç ãðóïïû, ñîñòî ùåé èç ñëåäóþùèõ ðàäèêàëîâ: Ñ2-Ñ12àëêèë, Ñ2-Ñ12àëêåíèë, Ñ2-Ñ12ãèäðîêñèàëêèë, Ñ2-Ñ12ãèäðîêñèàëêåíèë, Ñ2-Ñ12 àëêîêñèàëêèë, Ñ3-Ñ12öèêëîàëêèë, Ñ4-Ñ12öèêëîàëêèëàëêèë, Ñòðàíèöà: 1 RU 2 0 0 6 1 0 5 7 1 6 (86) Çà âêà PCT: US 2004/024541 (29.07.2004) R U (43) Äàòà ïóáëèêàöèè çà âêè: 10.09.2007 Áþë. ¹ 25 (72) Àâòîð(û): ÃØÂÅÍÄ Õàéíö Ó. (US), ÊÎÄÓÌÓÐÓ Âèøíóìóðòè (CA), ËÞ Øèôýí (CA), ÊÀÌÁÎÉ Ðàéýíäåð (CA) R 2 âûáèðàþò èç ãðóïïû, ñîñòî ùåé èç ñëåäóþùèõ ðàäèêàëîâ: Ñ2-Ñ12àëêèë, Ñ3-Ñ12àëêåíèë, Ñ2-Ñ12ãèäðîêñèàëêèë, Ñ2-Ñ12ãèäðîêñèàëêåíèë, Ñ2-Ñ12 àëêîêñèàëêèë, Ñ3-Ñ12öèêëîàëêèë, Ñ4-Ñ12öèêëîàëêèëàëêèë, Ñòðàíèöà: 2 A 2 0 0 6 1 0 5 7 1 6 R U A x è ó êàæäûé íåçàâèñèìî îçíà÷àåò 1, 2 èëè 3; W ïðåäñòàâë åò ñîáîé -Î-, -Ñ(O)O-, -N(R 1 ...

Pyridazine-3 (2H) -one derivatives and their use as PDE4 inhibitors

ÐÎÑÑÈÉÑÊÀß ÔÅÄÅÐÀÖÈß RU (19) (11) 2006 120 082 (13) A (51) ÌÏÊ C07D 237/22 (2006.01) ÔÅÄÅÐÀËÜÍÀß ÑËÓÆÁÀ ÏÎ ÈÍÒÅËËÅÊÒÓÀËÜÍÎÉ ÑÎÁÑÒÂÅÍÍÎÑÒÈ, ÏÀÒÅÍÒÀÌ È ÒÎÂÀÐÍÛÌ ÇÍÀÊÀÌ (12) ÇÀßÂÊÀ ÍÀ ÈÇÎÁÐÅÒÅÍÈÅ (21), (22) Çà âêà: 2006120082/04, 08.11.2004 (71) Çà âèòåëü(è): ÀËÜÌÈÐÀËÜ ÏÐÎÄÅÑÔÀÐÌÀ, Ñ.À. (ES) (30) Êîíâåíöèîííûé ïðèîðèòåò: 10.11.2003 ES P200302613 (43) Äàòà ïóáëèêàöèè çà âêè: 10.01.2008 Áþë. ¹ 1 (87) Ïóáëèêàöè PCT: WO 2005/049581 (02.06.2005) Àäðåñ äë ïåðåïèñêè: 101000, Ìîñêâà, Ì.Çëàòîóñòèíñêèé ïåð., 10, êâ.15, "ÅÂÐÎÌÀÐÊÏÀÒ", ïàò.ïîâ. È.À.Âåñåëèöêîé, ðåã. ¹ 11 R U PDE4 (57) Ôîðìóëà èçîáðåòåíè 1. Ïðîèçâîäíîå ïèðèäàçèíîíà ôîðìóëû (I) A 2 0 0 6 1 2 0 0 8 2 A (54) ÏÐÎÈÇÂÎÄÍÛÅ ÏÈÐÈÄÀÇÈÍ-3(2Í)-ÎÍÀ È ÈÕ ÏÐÈÌÅÍÅÍÈÅ Â ÊÀ×ÅÑÒÂÅ ÈÍÃÈÁÈÒÎÐΠãäå R 1 îçíà÷àåò: àòîì âîäîðîäà, ãðóïïó, âûáðàííóþ èç ñëåäóþùèõ ãðóïï: àöèë, àëêîêñèêàðáîíèë, êàðáàìîèë, ìîíîàëêèëêàðáàìîèë èëè äèàëêèëêàðáàìîèë; àëêèë, àëêåíèë èëè àëêèíèë, êîòîðûå íåîá çàòåëüíî çàìåùåíû îäíèì èëè áîëåå çàìåñòèòåë ìè, âûáðàííûìè èç ãðóïïû, âêëþ÷àþùåé ãàëîãåí, ãèäðîêñè, àëêîêñè, àðèëîêñè, àëêèëòèî, àðèëòèî, îêñî, àìèíî, ìîíî- èëè äèàëêèëàìèíî, àöèëàìèíî, ãèäðîêñèêàðáîíèë, àëêîêñèêàðáîíèë, êàðáàìîèë èëè ìîíî- èëè äèàëêèëêàðáàìîèë; àðèë èëè ãåòåðîàðèë, êîòîðûå íåîá çàòåëüíî çàìåùåíû îäíèì èëè áîëåå çàìåñòèòåë ìè, âûáðàííûìè èç ãðóïïû, âêëþ÷àþùåé ãàëîãåí, ãèäðîêñè, Ñòðàíèöà: 1 RU 2 0 0 6 1 2 0 0 8 2 (86) Çà âêà PCT: EP 2004/012604 (08.11.2004) R U (85) Äàòà ïåðåâîäà çà âêè PCT íà íàöèîíàëüíóþ ôàçó: 13.06.2006 (72) Àâòîð(û): ÄÀËÜ-ÏÈÀÇ Âèòòîðèî (IT), ÀÃÈËÀÐ-ÈÑÊÜÅÐÄÎ Íóðè (ES), ÁÓÈËÜ-ÀËÜÁÅÐÎ Ìàðè -Àíòîíè (ES), ÃÀÐÐÈÄÎ-ÐÓÁÈÎ Èîëàíäà (ES), ÄÆÎÂÀÍÍÎÍÈ Ìàðè -Ïàîëà (IT), ÃÐÀÑÈÀ-ÔÅÐÐÅÐ Õîðäè (ES), ËÓÌÅÐÀÑ-ÀÌÀÄÎÐ Âåíñåñëàî (ES), ÂÅÐÄÆÅËËÈ Êëàóäèà (IT) A 2 0 0 6 1 2 0 0 8 2 A R U 2 0 0 6 1 2 0 0 8 2 Ñòðàíèöà: 2 R U ãèäðîêñèàëêèë,ãèäðîêñèêàðáîíèë,àëêîêñè,àëêèëåíäèîêñè,àëêîêñèêàðáîíèë, àðèëîêñè, àöèë, àöèëîêñè, àëêèëòèî, àðèëòèî, àìèíî, íèòðî, öèàíî, ìîíî- èëè äèàëêèëàìèíî, àöèëàìèíî, êàðáàìîèë èëè ìîíî- èëè äèàëêèëêàðáàìîèë, äèôòîðìåòèë, ...

Pyridazine 3(2h) derivatives as inhibitor of phosphodiesterase 4 (pde4), method of their preparation, pharmaceutical composition and method of treatment

FIELD: chemistry. SUBSTANCE: invention refers to new pyridazine -3 (2H) derivatives, the chemical formula of which corresponds to the general formula , in which R 1 , R 2 , R 3 , R 4 and R 5 have values indicated in the formula of the invention. The compounds of the formula (I) are effective and selective inhibitors of phosphodiesterase 4. The invention also refers to the method of their preparation, pharmaceutical composition which includes these compounds, and to the application for medicine preparation for treatment of disease state or disease which medicable by meance of phosphodiesterase 4 inhibition. Besides, the object of the invention is the method of disease state and disease treatment by means of phosphodiesterase 4 inhibition. EFFECT: new compounds have effective biological properties. 19 cl, 25 tbl, 278 ex ÐÎÑÑÈÉÑÊÀß ÔÅÄÅÐÀÖÈß RU (19) (11) 2 326 869 (13) C2 (51) ÌÏÊ C07D 237/22 (2006.01) C07D 401/06 (2006.01) C07D 409/06 (2006.01) C07D 405/12 (2006.01) A61K 31/50 (2006.01) ÔÅÄÅÐÀËÜÍÀß ÑËÓÆÁÀ A61K 31/501 (2006.01) ÏÎ ÈÍÒÅËËÅÊÒÓÀËÜÍÎÉ ÑÎÁÑÒÂÅÍÍÎÑÒÈ,A61P 11/06 (2006.01) ÏÀÒÅÍÒÀÌ È ÒÎÂÀÐÍÛÌ ÇÍÀÊÀÌ A61P 17/06 (2006.01) A61P 19/02 (2006.01) A61P 1/08 (2006.01) (12) ÎÏÈÑÀÍÈÅ ÈÇÎÁÐÅÒÅÍÈß Ê ÏÀÒÅÍÒÓ (21), (22) Çà âêà: 2004136977/04, 14.05.2003 (24) Äàòà íà÷àëà îòñ÷åòà ñðîêà äåéñòâè ïàòåíòà: 14.05.2003 (30) Êîíâåíöèîííûé ïðèîðèòåò: 16.05.2002 (ïï.1-19) ES P200201111 (43) Äàòà ïóáëèêàöèè çà âêè: 10.07.2005 (45) Îïóáëèêîâàíî: 20.06.2008 Áþë. ¹ 17 (56) Ñïèñîê äîêóìåíòîâ, öèòèðîâàííûõ â îò÷åòå î ïîèñêå: WO 01/94319 A1, 13.12.2001, ðåôåðàò, ôîðìóëà èçîáðåòåíè ;. RU 2159236 Ñ2, 20.11.2000, ðåôåðàò, ôîðìóëà èçîáðåòåíè . (86) Çà âêà PCT: EP 03/05056 (14.05.2003) C 2 C 2 (85) Äàòà ïåðåâîäà çà âêè PCT íà íàöèîíàëüíóþ ôàçó: 16.12.2004 R U 2 3 2 6 8 6 9 (87) Ïóáëèêàöè PCT: WO 03/097613 (27.11.2003) Àäðåñ äë ïåðåïèñêè: 101000, Ìîñêâà, Ì.Çëàòîóñòèíñêèé ïåð., 10, êâ.15, "ÅÂÐÎÌÀÐÊÏÀÒ", ïàò.ïîâ. È.À.Âåñåëèöêîé, ðåã. ¹ 11 (54) ÏÐÎÈÇÂÎÄÍÛÅ ÏÈÐÈÄÀÇÈÍ-3(2H)-ÎÍÀ  ÊÀ×ÅÑÒÂÅ ÈÍÃÈÁÈÒÎÐΠ...

N-(4-pyridazinyl)-n'-phenylureas and -thioureas as well as plant growth regulators containing same

Urea compound or salt thereof

[Object] To provide a compound which can be used for the treatment of a disease associated with fatty acid amide hydrolase (FAAH), particularly urinary frequency, urinary incontinence and/or overactive bladder. [Means for solution] It is confirmed that a urea compound chemical-structurally characterized by having a piperidine or piperazine ring or a salt thereof has an excellent FAAH-inhibitory activity, and thus the present invention is completed. The urea compound or its pharmaceutically acceptable salt of the present invention can increase the effective bladder capacity and ameliorate the state of urinary frequency, and is therefore useful as an agent for treating urinary frequency, urinary incontinence and/or overactive bladder.

Urea compound or salt thereof

Urea compound or salt thereof

[PROBLEMS] To provide a compound which can be used for the treatment of a disease associated with fatty acid amide hydrolase (FAAH), particularly frequent urination, urinary incontinence and/or overactive bladder. [MEANS FOR SOLVING PROBLEMS] It is confirmed that an urea compound chemical-structurally characterized by having a piperidine or piperazine ring or a salt of the compound has a good FAAH-inhibiting activity. The urea compound or a pharmaceutically acceptable salt thereof can increase the effective bladder capacity and ameliorate the state of frequent urination, and is therefore useful as a therapeutic agent for frequent urination, urinary incontinence and/or overactive bladder.

Method of producing derivatives of 3(2n)-pyridazinone

A 3(2H)pyridazinone of the formula: <CHEM> wherein R1 is hydrogen, 2-propenyl or straight chained or branched C1-C4 alkyl; R2 is hydrogen or C1-C3 alkyl; X is chlorine or bromine; Y is hydrogen, nitro, -NHR3 wherein R3 is hydrogen or straight chained or branched C1-C4 alkyl, -AR4 wherein A is oxygen or sulfur and R4 is hydrogen, straight chained or branched C1-C6 alkyl, C3-C6 alkenyl having one double bond, C3-C6 alkynyl having one triple bond, phenyl or <CHEM> wherein R5 is hydrogen or C1-C4 alkyl, or halogen; Z1 is hydrogen, C1-C4 alkyl, -OR6 wherein R6 is hydrogen, straight chained or branched C1-C8 alkyl or <CHEM> wherein n is an integer of from 1 to 4, -N(R7)2 wherein R7 is C1-C4 alkyl, or halogen; Z2 is C1-C4 alkyl, -OR6 wherein R6 is as defined above, -N(R7)2 wherein R7 is as defined above, or halogen, provided that when R1 is straight chained or branched C2-C4 alkyl, Y is not hydrogen and when R1 is hydrogen, methyl or 2-propenyl, Y and R2 are not simultaneously hydrogen, or a pharmaceutically acceptable salt thereof.

Preparing method for 4-methyl 6-phenyl pyridazine

Pyridazines (I)[R=H,OH; R1=CH2CH2N(CH2CH2OX)Y; Y=H, alkyl or X+Y=ethylene were prepd. Thus, 3-chloro-4-methyl-6-phenylpyridazine was treated with HOCH2CH2NHCH2CH2NH2 to give (I)[R=H, R1= CH2CH2NHCH2CH2OH), which was reacted with ClCH2COCl to give 3-[2-(3- oxo-4-morpholinyl)ethylamino 4-methyl-6-phenylpyridazine (II). II had a ED50 in the reserpine ptosis antagonism test of 20mg/kg i.p. in mice and at 5.3 μmoles/kg i.p. in mice reduced ipsilateral rotations by 90%.

Glucokinase activating agents

FIELD: organic chemistry, biochemistry, medicine, endocrinology. SUBSTANCE: invention relates to compounds representing amide of the formula (I): wherein * means asymmetric carbon atom; R 1 and R 2 mean independently of one another hydrogen or halogen atom, amino-, hydroxyamino-, nitro-, cyano-, sulfonamido-group, (lower)-alkyl, -OR 5 , -C(O)OR 5 , perfluoro-(lower)-alkyl, (lower)-alkylthio-, perfluoro-(lower)-alkylthio-, (lower)-alkylsulfonyl-, perfluoro-(lower)-alkylsulfonyl-, or (lower)-alkylsulfinyl-group; R 3 means cycloalkyl comprising from 3 to 7 carbon atoms, or (lower)-alkyl comprising from 2 to 4 carbon atoms; R 4 means (O)NHR 40 or unsubstituted or monosubstituted five- or six-membered heteroaromatic ring bound by ring carbon atom with given amino-group wherein this five- or six-membered heteroaromatic ring comprises from 1 to 3 heteroatoms taken among sulfur, oxygen and nitrogen atoms and wherein one heteroatom represents nitrogen atom that is adjacent with connecting ring carbon atom; this monosubstituted heteroaromatic ring is monosubstituted by ring carbon atom that differs from adjacent atom with connecting carbon atom and substitute is taken among the following row including (lower)-alkyl, halogen atom, nitro-group, cyano-group, -(CH 2 ) n -OR 6 , -(CH 2 ) n -C(O)OR 7 , -(CH 2 ) n -C(O)NHR 6 , -C(O)-C(O)OR 8 and -(CH 2 ) n -NHR 6 , or its pharmaceutically acceptable salts. These compounds are activators of glucokinase that enhance secretion of insulin in treatment of diabetes mellitus of type II. EFFECT: valuable medicinal properties of compounds. 32 cl, 175 ex 2242469 С2 Ко РОССИЙСКАЯ ФЕДЕРАЦИЯ (19) Ри (0 э за д: за С2 хх К © А 5 Знубявковано на СО-ВОМ: МЕМОЗА КЕО ООД МЕРА ФЕДЕРАЛЬНАЯ СЛУЖБА ПО ИНТЕЛЛЕКТУАЛЬНОЙ СОБСТВЕННОСТИ (12) ИЗВЕЩЕНИЯ К ПАТЕНТУ НА ИЗОБРЕТЕНИЕ ММАА Досрочное прекращение действия патента из-за неуплаты в установленный срок пошлины за поддержание патента в силе Дата прекращения действия патента: 21.03.2011 Дата публикации: 27.01. ...

Method of producing 3-amino-4-methyl-6-phenylpyridazine

Изобретение относитс  к гетеро- циклическим соединени м, в частности к получению 3-амино-4-метил-6-фенйл- пиридазина (АМФП), обладающего пси хостимулирующим действием. Цель - получение более эффективных по активности соединений в указанном классе. Синтез АМФП ведут из З-хлор-4-метил- 6-фенилпиридазина и п тикратного избытка гидрата гидразина при кип чении 1,5 ч. Полученный 3-гидразино- 4-метил-6-фенилпиридазин гидрируют при 5 атм 48 ч в присутствии никел  Рене  в среде метанола или этанола. АМФП имеет т.пл. 130-132&amp;deg;С, брутто ф-ла С . Н N,,. АМФП может быть использован в терапии отклонений психомоторного поведени . По антидепрессивному и допаминомилитическоку действию АМФП близок к известному мина- прину, но менее токсичен ( АМФП 226 мг/кг, минаприна бЗмг/кР) и не оказьшает конвульсивного действи . 3 табл. § СО с 00 ел О5 QO О5 СМ The invention relates to heterocyclic compounds, in particular to the preparation of 3-amino-4-methyl-6-phenyl-pyridazine (AMPP), which has a psi-stimulating effect. The goal is to obtain more effective compounds in the specified class. The synthesis of AMPP is carried out from 3-chloro-4-methyl-6-phenylpyridazine and a five-fold excess of hydrazine hydrate at boiling for 1.5 hours. The obtained 3-hydrazino-4-methyl-6-phenylpyridazine is hydrogenated at 5 atm for 48 hours in the presence of nickel Rene in the environment of methanol or ethanol. AMPP has mp. 130-132 ° C, gross f-la C. N N ,,. AMPP can be used in the treatment of psychomotor abnormalities. By its antidepressant and dopamine-modicating effect, AMPP is close to the known minacan, but is less toxic (AMPP 226 mg / kg, minaprine bsmg / cP) and does not show a convulsive effect. 3 tab. § CO with 00 ate O5 QO O5 CM

Phtalazinon derivatives

There are according to the invention compounds of the formula I <IMAGE> in which A1 and A2 denote hydrogen, optionally substituted lower alkyl, lower alkenyl or lower alkynyl; heterocyclyl-lower alkyl, acyl, lower alkylsulphonyl or arylsulphonyl; or together denote optionally substituted lower alkylene; Ar1 and Ar2 denote aryl, heteroaryl or optionally substituted cycloalkyl; X stands for oxygen or sulphur; and in which Q denotes a bivalent radical of the formula <IMAGE> which is bonded via its Y-carrying carbon atom to the Q-bonding carbon atom and via its RB-carrying nitrogen atom to the RA-carrying nitrogen atom in formula I, in which Y stands for oxygen or sulphur and RA and RB denote hydrogen, optionally substituted lower alkyl or acyl; or in which Q denotes a bivalent radical of the formula <IMAGE> which is bonded by its carbon atom to the Q-bonding carbon atom and via its nitrogen atom to the RA-carrying nitrogen atom in formula I, where RA has the said meanings apart from acyl; salts thereof and tautomers thereof. These inhibit protein kinases, such as protein tyrosine kinases.

The method of obtaining 1- (3-trifluoromethylphenyl) -4,5-dichloropyridazone -6

Process for preparing 4,5-dichloro-phenyl-3-(2h)-pyridazinone

In a process for obtaining 4,5-dichloro-2-phenyl-3(2H)-pyridazinone from 5-chloro-4-amino-2-phenyl-3(2H)-pyridazinone the 5-chloro-4-amino-2-phenyl-3(2H)-pyridazinone is diazotized in a first stage in accordance with the following reaction: <IMAGE> (1) the compound (I) being obtained by dilution with water and filtration. In a second stage of the process the compound (I) is reacted with thionyl chloride in accordance with the following reaction: <IMAGE> (2) <IMAGE> the 4,5-dichloro-2-phenyl-3(2H)-pyridazinone being obtained by dilution with water and filtration.

Pyridazinylhydrazones,their preparation and pharmaceutical compositions containing them

Herbicide agent

Derivatives of 3(2h)-pyridazinone and their pharmaceutically acceptable salts and pharmaceutical composition on their base

FIELD: pharmaceutical industry. SUBSTANCE: derivatives of 3(2H)-pyridazinone having formula УтО0б0УбО0Сс П4 Го РОССИЙСКОЕ АГЕНТСТВО ПО ПАТЕНТАМ И ТОВАРНЫМ ЗНАКАМ (19) 13) ВУ” 2 054 004” Сл ОМ С 070 237/22, 401/12, 401/14, 403/12, 405/12, 409/42, 409/14, 413/12, 413/14, 417/12, Аб К 31/50 12) ОПИСАНИЕ ИЗОБРЕТЕНИЯ К ПАТЕНТУ РОССИЙСКОЙ ФЕДЕРАЦИИ (21), (22) Заявка: 5010505/04, 19.04.1991 (30) Приоритет: 25.04.1990 /Р 109914/90 (46) Дата публикации: 10.02.1996 (71) Заявитель: Ниссан Кемикал Индастриз Лтд. (4Р) (72) Изобретатель: Кейзо Таникава[Р], Акира Саито[Р], Такаси Матсумото[/Р], Риозо Сакода[Р], Нобутомо Тсурузое[/Р], Кен-ити (56) Ссылки: Европейская заявка ЕР М 0275997, кл. Сикада[Р] С 070 237/22, 1988. Европейская заявка ЕР М <“ 155798, кл. А 61К 31/50, 1985. Европейская (73) Патентообладатель: © заявка ЕР М 220044, кл. С 070 401/10, 1987. Ниссан Кемикап Индастриз Лтд. (УР) (86) Заявка РСТ: УР 9100517 (19.04.91) < © (54) ПРОИЗВОДНЫЕ 3(2Н)-ПИРИДАЗИНОНА ИЛИ ИХ ФАРМАЦЕВТИЧЕСКИ ПРИЕМЛЕМЫЕ СОЛИ И ФАРМАЦЕВТИЧЕСКАЯ КОМПОЗИЦИЯ НА ИХ ОСНОВЕ <> (57) Реферат: фармацевтически приемлемую соль в < Использование: в количестве 0,5 - 95 мас.%. 2 с. п. Фф-пы. о химико-фармацевтической промышленности. Структура соединения ф-лы 1: Сущность изобретения: — производные о © 1 3(2Н)пиридазинона — Фф-плы 1 или их Е фармацевтически приемлемые соли при “Н с определенных значениях радикалов и | | р фармацевтическая композиция, обладающая М, | противотромбической, инотропной, —СН-Аг > сосудорасширяющей и антагонистической по 2 |3 отношению к медиатору — активностью, ОЕ Е 0 содержащая В качестве активного ингредиента соединение ф-лы 1 или его 10 ил., 12 табл. УтО0б0УбО0Сс П4 Го (19) 13) ВУ” 2 054 004” Сл о © 070 237/22, 401/12, 401/14, 403/12, 405/42, 409/12, 409/14, 413/12, 413/14, 417/12, А 61 К 31/50 КУЗЗАМ АСЕМСУ ГОК РАТЕМТ$ АМО ТКАОЕМАКК$ 12) АВЗТКАСТ ОЕ 1МУЕМТОМ (21), (22) АррИсаНоп: 5010505/04, 19.04.1991 (71) АррИсапе: М№!5зап КептиКа! пдазмх Ша. (}Р) (30) Рпощу: 25.04.1990 УР ...

Method of isolation of residual substances from sewage in synthesis of 5-amino- 4-chloro-2-phenyl-3(2h)-pyridazinone

FIELD: sewage treatment. SUBSTANCE: method involves separation and repeated utilization of residual substances from sewage in synthesis of 5-amino-4-chloro-2-phenyl-3(2H)-pyridazinone. The latter compound is synthesized from 4,5-dichloro-2-phenyl-3(2H)-pyridazinone and ammonia. Sewage is acidified up to pH 1-4, and formed precipitate is removed. Precipitate is converted to 4,5-dichloro-2-phenyl-3(2H)-pyridazinone by chlorination. Acidification is made with mineral acid and chlorination is carried out with phosphorus oxychloride at 90-120 C under pressure 1-30 bars. EFFECT: improved method of isolation. 5 cl 690 г0с ПЧ Го РОССИЙСКОЕ АГЕНТСТВО ПО ПАТЕНТАМ И ТОВАРНЫМ ЗНАКАМ (19) (51) МПК ВИ “” 2010 769‘ 13) Сл С 02 Е 1/58 12) ОПИСАНИЕ ИЗОБРЕТЕНИЯ К ПАТЕНТУ РОССИЙСКОЙ ФЕДЕРАЦИИ (21), (22) Заявка: 4830755/26, 15.08.1990 (30) Приоритет: 0Е/16.08.89/3926905 (30) Приоритет: 16.08.1989 ОЕ 89 3926905 (46) Дата публикации: 15.04.1994 (71) Заявитель: БАСФ АГ (ОЕ) (72) Изобретатель: Валтер Траутманн[0Е], Хельмут Фрелих[ОЕ], Волфганг Милднер[ОЕ] (73) Патентообладатель: БАСФ АГ (ОЕ) (54) СПОСОБ ВЫДЕЛЕНИЯ ОСТАТОЧНЫХ ВЕЩЕСТВ ИЗ СТОЧНЫХ ВОД СИНТЕЗА 5-АМИ- НО-4-ХЛОР-2-ФЕНИЛ-3(2Н)-ПИРИДАЗИНОНА (57) Реферат: Изобретение относится к способам отделения и повторного использования остаточных веществ из сточной воды синтеза 5-амино-4-хлор-2-фенил-3-(2Н)-пиридазинона, полученного из 4, 5-дихлор-2-фенил-3-(3ЗН)-пиридазинона и аммиака, путем подкисления сточных вод до рН 1 - 4 и удалением образующегося осадка, который переводят посредством хлорирующего средства В 4,5-дихлор-2-фенил-3(2Н)-пиридазинон. Подкислением ведут минеральной кислотой, а хлорирование осуществляют фосфорокислохлоридом при 90 - 120С и при давлении 1 - 30 бар. 4 3. п. ф-лы. 2010769 С1 КО 690 г0с ПЧ Го КУЗЗАМ АСЕМСУ ГОК РАТЕМТ$ АМО ТКАОЕМАКК$ (19) ВИ “” 2010 769‘ 13) СЛ (51) 1пЁ. С1.5 С 02Е 1/58 12) АВЗТКАСТ ОЕ 1МУЕМТОМ (21), (22) АррИсаНоп: 4830755/26, 15.08.1990 (30) Рпошу: ОЕ6.08.89/3926905 (30) Рпогйу: 16.08.1989 ОЕ 89 ...

Heteroaromatic glucokinase activators

2,3-Di-substituted N-heteroaromatic propionamides with said substitution at the 3-position being a substituted phenyl group and at the 2-position being a methyl cycloalkyl ring, said propionamides being glucokinase activators which increase insulin secretion in the treatment of type II diabetes.

Heteroaromatic glucokinase activators

2,3-Di-substituted N-heteroaromatic propionamides with said substitution at the 2-position being a substituted phenyl group and at the 3-position being a cycloalkyl ring, said propionamides being glucokinase activators which increase insulin secretion in the treatment of type II diabetes.

Preventives or remidies for alzheimer's disease or amyloid protein fibrosis inhibitors containing nitrogen-containing heteroaryl compounds

The present invention relates to preventives or remedies for Alzheimer's disease, or to amyloid protein fibril-formation inhibitors, which include as an active ingredient a compound of general formula (I) below or a pharmacologically permitted salt thereof; and also to nitrogen-containing heteroaryl derivatives having specific substituents, or pharmacologically permitted salts thereof, which are valuable as preventives or remedies for Alzheimer's disease, or as amyloid protein fibril-formation inhibitors: (where, R 1 and R 2 are H or alkyl; Z 1 and Z 2 are H, alkyl, alkoxy, haloalkyl or halogeno; Z 3 is alkoxy, SH, alkylthio, NH 2 , mono- or di-alkylamino, OH or halogeno; Z 4 and Z 5 are H or halogeno; and A is 4,6-pyrimidine-1,3-diyl, 1,3,5-triazine-2,6-diyl, etc).

Preventives or remedies for alzheimer's disease or amyloid protein fibrosis inhibitors containing nitrogen-containing heteroaryl compounds

本发明涉及含有具有下述通式(I)的化合物或其药理学上允许的盐作为有效成分的阿耳茨海默氏病的预防药或治疗药或者淀粉样蛋白纤维化抑制剂，以及作为阿耳茨海默氏病的预防药或治疗药或者淀粉样蛋白纤维化抑制剂有用的具有特定取代基的含氮芳香杂环衍生物或其药理学上允许的盐。(式中，R 1 、R 2 ：H、烷基；Z 1 、Z 2 ：H、烷基、烷氧基、卤代烷基、卤素；Z 3 ：烷氧基、SH、烷硫基、NH 2 、一或二烷基氨基、OH、卤素；Z 4 、Z 5 ：H、卤素；A：4，6－嘧啶－1，3－二基、1，3，5－三嗪－2，6－二基等)。

Herbicide composition

Patent RU2016142611A3

`”ВУ“” 2016142611” АЗ Дата публикации: 26.12.2018 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 2016142611/04(068232) 27.03.2015 РСТД52015/022868 27.03.2015 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. 61/973,689 01.04.2014 05 Название изобретения (полезной модели): [Х] - как заявлено; [ ] - уточненное (см. Примечания) ПРОЛЕКАРСТВЕННЫЕ СРЕДСТВА ИНГИБИТОРОВ ОБРАТНОЙ ТРАНСКРИПТАЗЫ ВИЧ Заявитель: МЕРК ШАРП И ДОУМ КОРЦП., 05 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) СО7Е 9/65568 (2006.01) Аб1К 31/662 (2006.01) Аб1Р 31/18 (2006.01) 5. ОБЛАСТЬ ПОИСКА 5.1 Проверенный минимум документации РСТ (указывается индексами МПК) СО7Е 9/6558, Аб1К 31/662, Аб1Р 31/18 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): СТРО, РЕРАТБпе, ОУ/Р1, ЕАРАТТ$, Езрасепеь, 7-Р1а Раб, К-РТОМ, Рабеагсв, КОРТО, Кеахуз, 5ТРО, 5ТМ Оппе, ОЗРТО 6. ДОКУМЕНТЫ, ОТНОСЯЩИЕСЯ К ПРЕДМЕТУ ПОИСКА Кате- ...

Anti-virally active pyridazinamines

Pyridazinamines of the formula and their pharmaceutically acceptable acid addition salts and/or possible stereochemically isomeric forms and/or tautomeric forms for use as medicines in particular for use as anti-viral agents; pharmaceutical compositions containing such compounds as an active ingredient and a method of preparing such compositions; novel pyridazinamines of the fnrmula and a method of preparing said compounds

Carboxylic acid derivatives that inhibit the binding of integrins to their receptors and pharmaceutical compositions comprising the same

α 4 β 1 인테그린이 이의 수용체, 예를 들면 VCAM-1(혈관 세포 흡착 분자-1) 및 피브로넥틴에 결합하는 것을 억제하는 방법; 이러한 결합을 억제하는 화합물; 이러한 화합물을 함유하는 약제학적 활성 조성물; 및 α 4 β 1 이 관련된 질병 상태를 억제 또는 예방하기 위한 상기와 같은 이러한 화합물 또는 제형의 용도가 본원에 기술되어 있다. a method of inhibiting α 4 β 1 integrins from binding to their receptors such as VCAM-1 (vascular cell adsorption molecule-1) and fibronectin; Compounds which inhibit this binding; Pharmaceutically active compositions containing such compounds; And the use of such compounds or formulations as described above for inhibiting or preventing a disease condition involving α 4 β 1 . α4β1 인테그린, α4β1 인테그린의 수용체, VCAM-1, 피브로넥틴, 카복실산 유도체 α4β1 integrin, receptor of α4β1 integrin, VCAM-1, fibronectin, carboxylic acid derivative

Method of producing pyridazineamines or pharmaceutically acceptable salts of acids thereof,or stereochemical isomers thereof,or tautomers thereof

Pyridazinamines of the formula and their pharmaceutically acceptable acid addition salts and/or possible stereochemically isomeric forms and/or tautomeric forms for use as medicines in particular for use as anti-viral agents; pharmaceutical compositions containing such compounds as an active ingredient and a method of preparing such compositions; novel pyridazinamines of the fnrmula and a method of preparing said compounds

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.

Preventives or remedies for alzheimer's disease or amyloid protein fibrosis inhibitors containing nitrogen-containing heteroaryl compounds

본 발명은 하기 화학식(Ⅰ)을 갖는 화학물 또는 이의 약물학적으로 허용되는 염을 유효성분으로서 포함하는, 알츠하이머병의 예방약 또는 치료약 또는 아밀로이드 단백질 섬유화 억제제 및 알츠하이머병의 예방약 또는 치료약 또는 아밀로이드 단백질 섬유화 억제제로서 유용한 특정 치환기를 갖는 질소함유 헤테로아릴 유도체 또는 이의 약리학적으로 허용되는 염에 관한 것이다: The present invention comprises a chemical having the formula (I) or a pharmacologically acceptable salt thereof as an active ingredient, a prophylactic or therapeutic drug for Alzheimer's disease or an amyloid protein fibrosis inhibitor and a prophylactic or therapeutic drug for Alzheimer's disease or an amyloid protein fibrosis inhibitor A nitrogen-containing heteroaryl derivative or pharmacologically acceptable salt thereof having a specific substituent useful as: (상기 식에서, R 1 , R 2 :H, 알킬; Z 1 , Z 2 :H, 알킬, 알콕시, 할로겐화알킬, 할로겐; Z 3 :알콕시, SH, 알킬티오, NH 2 , 모노- 또는 디알킬아미노, OH, 할로겐; Z 4 ,Z 5 :H, 할로겐; A:4,6-피리미딘-1,3-디일, 1,3,5-트리아진-2,6-디일 등임). Wherein R 1 , R 2 : H, alkyl; Z 1 , Z 2 : H, alkyl, alkoxy, halogenated alkyl, halogen; Z 3 : alkoxy, SH, alkylthio, NH 2 , mono- or dialkylamino , OH, halogen; Z 4 , Z 5 : H, halogen; A: 4,6-pyrimidine-1,3-diyl, 1,3,5-triazine-2,6-diyl and the like).

Process for the preparation of pure 4-amino-5-halogen-pyridazonen- (6)

Pyridazinone hydrochloride compound and method for producing the same

The present invention relates to a 3/2-hydrochloride of 4-chloro-5-[3- (4-benzylpiperazin-1- yl)carbonylmethoxy-4- methoxybenzylamino]- 3(2H)-pyridazinone, and also relates to a method for producing the 3/2- hydrochloride of 4-chloro-5-[3- (4-benzylpiperazin-1- yl)carbonylmethoxy-4- methoxybenzylamino]- 3(2H)-pyridazinone which comprises crystallizing in an alcohol type solvent or an alcohol type-ester type mixture solvent in the presence of hydrogen chloride and water.

Pyridazinone derivative

내용없음 No content

Pyridazinone derivative

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

Substituted 6-(1-piperazinyl)-pyridazines as 5-ht6 receptor antagonists

FIELD: chemistry. SUBSTANCE: invention relates to novel substituted 6-(1-piperazinyl)-pyridazines of formula , where R 1 is chlorine, trifluoromethyl or cyano; R 2 is phenyl or phenyl substituted with a halogen; R* 1 is hydrogen, C 1-4 -alkyl or pyridinylmethyl; X is -O-, -NH-, -CH 2 -, -CH(OH)-, -SO 2 -, -CO-, -NH-CH 2 -, -O-CH 2 -, 1,2-ethendiyl or ethyndiyl; or a pharmaceutically acceptable addition salt or solvate thereof as well as pharmaceutical compositions containing said novel compound as an active ingredient. EFFECT: improved properties of derivatives. 8 cl, 4 tbl, 6 ex РОССИЙСКАЯ ФЕДЕРАЦИЯ (19) RU (11) 2 502 734 (13) C2 (51) МПК ФЕДЕРАЛЬНАЯ СЛУЖБА ПО ИНТЕЛЛЕКТУАЛЬНОЙ СОБСТВЕННОСТИ (12) ОПИСАНИЕ C07D C07D C07D C07D A61K A61P A61P 237/00 (2006.01) 237/18 (2006.01) 237/22 (2006.01) 403/04 (2006.01) 31/501 (2006.01) 3/04 (2006.01) 25/28 (2006.01) ИЗОБРЕТЕНИЯ К ПАТЕНТУ (21)(22) Заявка: 2011103759/04, 01.07.2009 (24) Дата начала отсчета срока действия патента: 01.07.2009 2 5 0 2 7 3 4 R U (85) Дата начала рассмотрения заявки PCT на национальной фазе: 03.02.2011 C 2 C 2 (56) Список документов, цитированных в отчете о поиске: WO 03/072548 A1, 04.09.2003. HOLENZ et al. "Medicinal chemistry strategies to 5-TH6 receptor ligands as potential cognitive enhancers and antiobesity agents". DRUG DISCOVERY TODRY, ELSEVIER, RAHWAY, vol.11. no.7-8, 2006. p.p.283-299. RU 2326118 C2, 10.06.2008. (86) Заявка PCT: EP 2009/004745 (01.07.2009) (87) Публикация заявки РСТ: WO 2010/000456 (07.01.2010) Адрес для переписки: 129090, Москва, ул. Б.Спасская, 25, стр.3, ООО "Юридическая фирма Городисский и Партнеры", пат.пов. Е.Е.Назиной, рег.№ 517 (54) ЗАМЕЩЕННЫЕ 6-(1-ПИПЕРАЗИНИЛ)-ПИРИДАЗИНЫ В КАЧЕСТВЕ АНТАГОНИСТОВ 5НТ6 РЕЦЕПТОРА (57) Реферат: Изобретение относится к новым замещенным 6-(1-пиперазинил)-пиридазинам формулы (I), Где R 1 является хлором, трифторметилом или циано; R 2 является фенилом или фенилом, замещенным галогеном; R3 является или водородом, C1 ‐ 4-алкилом пиридинилметилом ...

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 FR2189406B1

Process for preparing 3-sulfanilamido-6-methoxy-pyridazine

New 3-alkyl-pyridazones and their preparation process

Herbicide

NOVEL BIAROMATIC COMPOUNDS THAT ACTIVATE PPAR-GAMMA TYPE RECEPTORS AND THEIR USE IN COSMETIC OR PHARMACEUTICAL COMPOSITIONS

L'invention concerne de nouveaux composés bi-aromatiques qui répondent à la formule générale (I) suivante : (CF DESSIN DANS BOPI) ainsi que leur méthode de préparation, et leur utilisation dans des compositions pharmaceutiques destinées à un usage en médecine humaine ou vétérinaire (en dermatologie, ainsi que dans le domaine des maladies cardio-vasculaires, des maladies immunitaires et/ou des maladies liées au métabolisme des lipides), ou bien encore dans des compositions cosmétiques. The invention relates to new bi-aromatic compounds which correspond to the following general formula (I): (CF DRAWING IN BOPI) as well as their method of preparation, and their use in pharmaceutical compositions intended for use in human or veterinary medicine (in dermatology, as well as in the field of cardiovascular diseases, immune diseases and / or diseases linked to lipid metabolism), or even in cosmetic compositions.

New sulfanilaminopyridazine derivatives and their preparation process

DERIVATIVES OF PHENYL-1 DIHYDRO 1-4-ARYLALCOYLAMINO-3-OXO-4-PYRIDAZINES, THEIR PREPARATION AND THEIR USE IN THERAPEUTICS.

1-phenyl 1,4-dihydro 3-arylalkylamino 4-oxo pyridazines having geeral formula (I). Pharmaceutical compositions containing at least one of the compounds of general formula (I) as the active principle are also provided.

Glucokinase activators

The present invention relates to compounds of formula (I) wherein R1, R2, R3 and R4 are as defined in claim 1 and pharmaceutically acceptable salts thereof. The compounds are glucokinase activators which increase insulin secretion in the treatment of type II diabetes.

Patent FR2348920B1

Herbicide

Process for the preparation of new 3-amino-pyridazines substituted in position 6

Process for the preparation of 4-amino-5-halogeno-6-pyridazones

NOVEL PHENOLIC DERIVATIVES, AND THEIR PHARMACEUTICAL OR COSMETIC USE

La présente invention a pour objet de nouveaux composés de formule générale : et leur utilisation cosmétique ou pharmaceutique. The present invention relates to novel compounds of general formula: and their cosmetic or pharmaceutical use.

Patent FR2432020B1

NEW PYRIDAZINYLHYDRAZONES, THEIR PREPARATION PROCESS AND NEW MEDICINAL PRODUCTS CONTAINING THESE COMPOUNDS

La présente invention a pour objet de nouvelles pyridazinyl-hydrazones qui répondent à la formule générale I ci-dessous et les sels compatibles du point de vue pharmaceutique de ces composés. Ces composés sont obtenus à partir d'un composé de formule générale IV ci-dessous, soit par réaction avec une cétone appropriée, soit par réaction avec un acide approprié et traitement de l'acide obtenu par un alcool, soit par réaction avec un ester approprié. Application des pyridazinylhydrazones conformes à l'invention en tant que médicaments hypotenseurs. The subject of the present invention is new pyridazinyl-hydrazones which correspond to the general formula I below and the pharmaceutically compatible salts of these compounds. These compounds are obtained from a compound of general formula IV below, either by reaction with an appropriate ketone, or by reaction with an appropriate acid and treatment of the acid obtained with an alcohol, or by reaction with an ester appropriate. Application of the pyridazinylhydrazones in accordance with the invention as hypotensive drugs.

Process for the preparation of 1, 3-diaryl-5-amino-pyridazones- (6)

Herbicidal pyridazone derivs - n-(1-(3-trifluoromethylphenyl) -5-halo-pyridazone-6-yl-4)-n'-sulphonyl-(thio)ureas

Cpds. (I):- (where X is halogen; Y is O or S; R1 is 1-4C alkyl; R2 is H or 1-4C alkyl; and R3 is 1-4C alkyl, cycloalkyl, heterocyclyl or phenyl opt. substd. by halogen, alkyl, alkoxy, haloalkyl or NO2) are prepd. by treating a 1-(3-trifluorophenyl)-5-halo-4-amino-pyridazone-6 with a sulphonyl iso(thio)cyanate and opt. alkylating the product to introduce R2.

CNS depressant 5-(1-methylhydrazino)-substd. pyridazinone deriv. - from methyl-hydrazine and corresp 5-halo substd pyridazinone deriv

Pyridazone derivs of formula (I) (where X is are new and may be prepd. from (I; X =F, Cl or Br) by reaction with methylhydrazine. (I) possess CNS depressant, esp. minor tranquilliser, anticonvulsant and sedative-hypnotic activities.

Patent JPS56501486A

Process for the preparation of new derivatives of pyridazon- (6)

2H PYRIDAZIN-3-ONES DERIVATIVES, THEIR PREPARATION AND THEIR APPLICATION IN HUMAN THERAPEUTICS

NEW TRIAZAPENTADIENES, THEIR PREPARATION PROCESS AND THEIR APPLICATION AS ACARICIDES

DERIVATIVES OF OXADIAZOLES AND PYRIDAZINES, THEIR PREPARATION AND THEIR THERAPEUTIC APPLICATION

Products affecting plant growth

NOVEL PHENOLIC DERIVATIVES, AND THEIR PHARMACEUTICAL OR COSMETIC USE

Pyridazinone derivatives with pharmaceutical activity

식 (I)의 3(2H)-피리다지논 유도체, 이의 염, 이의 제조 방법 및 이를 함유하는 약학적 조성물 : 3 (2H) -pyridazinone derivatives of formula (I), salts thereof, methods for their preparation and pharmaceutical compositions containing them: 〔식중, 상호 독립적인 각각의 R 1 , R 2 및 R 3 는 수소원자 또는 C 1-4 알킬기이고, X는 염소 원자 또는 브롬 원자이며, Y 1 는 수소 원자, 할로겐원자, 니트로기, 아미노기 또는 C 1-4 알콕시기이고, Y 2 는 수소 원자, 할로겐 원자, 히드록실기, C 1-4 알킬기 또는 C 1-4 알콕시 이며, 또는 히드록실기로 치환될 수 있는 C 1-5 알킬렌 사슬이고, B는 카르보닐기 또는 C 1-4 알킬기로 치환될 수 있는 메틸렌 사슬이며, 상호 독립적인 각각의 R 4 및 R 5 는 C 1-4 알킬기이거나, 또는 R 4 는 수소 원자이고 R 5 는 Z-Ar (식중, Z는 C 1-5 알킬렌 사슬이고, Ar는 질소 원자를 포함할 수 있는 방향족 6-원 고리이다.) 이거나, 또는 R 4 및 R 5 는 함께 C 2-6 고리 알킬렌기를 형성하거나, 또는 R 4 및 R 5 는 인접한 질소와 함께 식 (a)의 4-치환된 피페라진 고리 (식중, R 6 은 C 1-4 알킬이기다.)를 형성한다.〕. [Wherein, each independently of each other, R 1 , R 2 and R 3 are a hydrogen atom or a C 1-4 alkyl group, X is a chlorine atom or a bromine atom, Y 1 is a hydrogen atom, a halogen atom, a nitro group, an amino group or A C 1-4 alkoxy group, Y 2 is a hydrogen atom, a halogen atom, a hydroxyl group, a C 1-4 alkyl group or a C 1-4 alkoxy, or a C 1-5 alkylene chain which may be substituted with a hydroxyl group B is a methylene chain which may be substituted with a carbonyl group or a C 1-4 alkyl group, and each of R 4 and R 5 , which are independent of each other, is a C 1-4 alkyl group, or R 4 is a hydrogen atom, and R 5 is Z- Ar (wherein Z is a C 1-5 alkylene chain and Ar is an aromatic 6-membered ring which may contain nitrogen atoms) or R 4 and R 5 together represent a C 2-6 ring alkylene group forming, or R 4 and R 5 is a 4-substituted piperazine ring of formula (a) together with the adjacent nitrogen to form a (wherein, R 6 is. C 1-4 alkyl win) ...

Pyridazine derivatives

Herbicides