ПИПЕРИДИНИЛПИРАЗОЛОПИРИМИДИНОНЫ И ИХ ПРИМЕНЕНИЕ

FIELD: chemistry. SUBSTANCE: present invention relates to novel substituted piperidinylpyrazolopyrimidinones, having structural formula (I-A), in which radicals and symbols have the definitions given in the claim, methods for preparing them, based medicinal agents, use thereof in a method of treating and/or preventing diseases. EFFECT: compounds can be used for treating and/or preventing acute and recurrent haemorrhage in patients with underlying hereditary or acquired haemostatic disorders or without them, where haemorrhage is associated with a disease or medical intervention selected from a group including severe menstrual bleeding, postpartum haemorrhage, haemorrhoid shock, haemorrhagic cystitis, gastrointestinal bleeding, trauma, surgical intervention, transplantation, stroke, liver disease, hereditary angioedema, nosebleed and synovitis and cartilage damage following haemarthrosis. 18 cl, 4 tbl, 472 ex РОССИЙСКАЯ ФЕДЕРАЦИЯ (19) RU (11) (13) 2 713 937 C2 (51) МПК C07D 487/04 (2006.01) A61K 31/519 (2006.01) A61K 31/5377 (2006.01) A61K 31/541 (2006.01) A61K 45/06 (2006.01) A61P 7/04 (2006.01) ФЕДЕРАЛЬНАЯ СЛУЖБА ПО ИНТЕЛЛЕКТУАЛЬНОЙ СОБСТВЕННОСТИ (12) ОПИСАНИЕ ИЗОБРЕТЕНИЯ К ПАТЕНТУ (52) СПК C07D 487/04 (2019.05); A61K 31/519 (2019.05); A61K 31/5377 (2019.05); A61K 31/541 (2019.05); A61K 45/06 (2019.05); A61P 7/04 (2019.05) (21)(22) Заявка: 2017119419, 30.10.2015 30.10.2015 Дата регистрации: 11.02.2020 03.11.2014 EP 14191410.1; 30.04.2015 EP 15165918.2 (43) Дата публикации заявки: 05.12.2018 Бюл. № 34 (45) Опубликовано: 11.02.2020 Бюл. № 5 (86) Заявка PCT: EP 2015/075208 (30.10.2015) R U 2 7 1 3 9 3 7 (87) Публикация заявки PCT: WO 2016/071216 (12.05.2016) Адрес для переписки: 105064, Москва, а/я 88, "Патентные поверенные Квашнин, Сапельников и партнеры" (73) Патентообладатель(и): БАЙЕР ФАРМА АКЦИЕНГЕЗЕЛЬШАФТ (DE) (56) Список документов, цитированных в отчете о поиске: WO 2014/173289 A1, 30.10.2014. WO 2012/047156 A1, 12.04.2012. WO 2014/012964 A1, 23.01.2014. RU ...

ПИРАЗОЛО[3,4-С]ПИРИДИНЫ И СПОСОБЫ ИХ ПРИМЕНЕНИЯ

... 1. Соединение, выбранное из формулы I:и его стереоизомеры, геометрические изомеры, таутомеры или фармацевтически приемлемые соли, где:Rвыбирают из -CN, -CHCN, -CHCONH, -CONH, -CONHCH, -CON(СН), -NHCONH, C-C-карбоциклила, C-C-гетероциклила, C-C-гетероарила, -(C-C-гетероарил)-(C-C-гетероарила), -(C-C-гетероарил)-(C-C-гетероциклила), -(C1-C-гетероарил)-O-(C-C-гетероциклила), -(C-Cгетероарил)-O-(C-C-алкилен)-(C-C-гетероциклила), -(C-C-гетероарил)-NR-(C-C-гетероциклила) и -(C-C-гетероарил)-NR-(C-C-алкилен)-(C-C-гетероциклила);Rвыбирают из C-C-алкила, C-C-карбоциклила, C-C-гетероциклила, C-C-гетероарила, C-C-арила, -(C-C-арил)-(C-C-гетероциклила), -(C-C-алкилен)-(C-C-гетероциклила), -(C-C-алкилен)-NR(C-C-гетероциклила), -(C-C-алкилен)-NR-(C-C-алкилен)-(C-C-гетероциклила), -(C-C-гетероарил)-(C-C-гетероарила), -(C-C-гетероарил)-(C-C-гетероциклила), -(C-C-гетероарил)-(C-C-гетероциклил)-(C-C-гетероциклила), -(C-C-гетероарил)-NR-(C-C-гетероциклила), -(C-C-гетероарил)-(C-C-алкилен)-(C-C-гетероциклила ...

SUBSTITUTED BENZAMIDES FOR TREATING ARTHROPODES

Indazole derivatives.

The invention relates to a vaccine composition comprising an antigen, an immunoiogically active saponin fraction and a sterol.

Indazole derivatives

SUBSTITUTED BENZAMIDES FOR TREATING ARTHROPODES

SUBSTITUTED BENZAMIDES FOR TREATING ARTHROPODES

SUBSTITUTED ARYLPYRAZOLE AS PARASITIZIDE

PYRAZOLE SEKRETORI PHOSPHOLIPASE-A2-INHIBITOREN NOT PANKREATI AS HUMAN ONES

SUBSTITUTED PYRAZOLE HERBICIDES

A pyrazole compound having the structural formula wherein R1is C1-C4 haloalkyl or ROR5, wherein R is C1-C2 alkylene or C2 alkylidene and R5 is hydrogen, C1-C4 alkyl, C2-C5 alkanoyl, aroyl, C8-C10 aralkanoyl, C7-C9 aralkyl, pnenyl, phenyl substituted with C1-C4 alkyl, C1-C4 alkoxy, trihalomethyl, hydroxy, cyano or nitro, or benzoyl substituted with halogen, C1-C4 alkyl, C1-C4 alkoxy, trihalomethyl, hydroxy, cyano or nitro; R2 is C1-C4 alkyl, C5-C6 cycloalkyl, C7-C9 aralkyl, C7-C9 alkaryl, phenyl, naphthyl, a 5- or 6-membered heterocyclic group containing oxygen, sulfur or nitrogen, or phenyl substituted with halogen, trihalomethyl, C1-C4 alkoxy, hydroxy or cyano; Y is oxygen or sulfur; R3 is C1-C4 alkyl, C2-C4 alkenyl, C3-C4 alkynyl, C2-C6 alkoxyalkyl or C2-C6 alkylthioalkyl; R4 is hydrogen, C1-C4 alkyl or trihalomethyl; provided that R2 is not 3,4-dialkylphenyl or 3,4-dihalophenyl useful as a herbicide is disclosed.

PYRAZOLINE INSECTICIDES

... 1) Insecticidal compounds of formula I < IMG > I where R1 is hydrogen, alkyl or alkenyl; X is oxygen or sulphur; each R2, which may be the same or different, if halogen, alkyl, haloalkyl, cyano, nitro, alkoxy, haloalkoxy, alkylthio, haloalkylthio, alkylsulphonyloxy, alkylsulphonyl, alkoxycarbonyl or acyl or two adjacent R2 groups together with the carbons to which they are attached form a 1,3-dioxolane ring. m is 0 to 4; either a) Ra is hydrogen and one of Rb and Rc is phenyl, para substituted by the group R4, and the other is hydrogen; or b) Ra and Rb are both alkyl and Rc is phenyl para substituted by the group R4; R4 and R5 which may be the same or different, are R8SO2O, hydrogen, halogen, alkyl, haloalkoxy, alkylthio or alkylsulphonyl, wherein R8 is alkyl or haloalkyl; with the proviso that at least one of R4 and R5 is R8SO2O or at least R4 is haloalkoxy.

SUBSTITUTED BENZAMIDES FOR THE TREATMENT OF ARTHROPODS

Substituted arylpyrazoles

This invention relates to a range of 1-aryl-4-cyclopropylpyrazoles in which there is at least one fluorine attached to the cyclopropyl ring, to compositions comprising such compounds, processes to their synthesis and their use as parasiticides.

4-(4-Метоксифенилдиазенил)-3,5-диметил-1-(4-нитрофенил)-1H-пиразол с антимикотической активностью в отношении штаммов патогенных грибов - дерматофитов

Изобретение направлено на создание препаратов для лечения грибковых заболеваний на основе органических соединений. Предложен 4-(4-метоксифенилдиазенил)-3,5-диметил-1-(4-нитрофенил)-1H-пиразол. Технический результат заключается в получении 4-(4-метоксифенилдиазенил)-3,5-диметил-1-(4-нитрофенил)-1Н-пиразола, обладающего высокой антимикотической активностью в отношении инфекций, вызванных штаммами патогенных грибов – дерматофитов. 1 табл., 8 пр.

Patent RU2017119419A3

ВУ” 2017119419`” АЗ Дата публикации: 10.06.2019 Форма № 18 ИЗПМ-2011 Федеральная служба по интеллектуальной собственности Федеральное государственное бюджетное учреждение 5 «Федеральный институт промышленной собственности» (ФИПС) ОТЧЕТ О ПОИСКЕ 1. . ИДЕНТИФИКАЦИЯ ЗАЯВКИ Регистрационный номер Дата подачи 2017119419/04(033710) 30.10.2015 РСТ/ЕР2015/075208 30.10.2015 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. 14191410.1 03.11.2014 ЕР* 2. 15165918.2 30.04.2015 ЕР* Название изобретения (полезной модели): [Х] - как заявлено; [ ] - уточненное (см. Примечания) ПИПЕРИДИНИЛПИРАЗОЛОПИРИМИДИНОНЫ И ИХ ПРИМЕНЕНИЕ Заявитель: БАЙЕР ФАРМА АКЦИЕНГЕЗЕЛЬШАФТ, ОЕ 2. ЕДИНСТВО ИЗОБРЕТЕНИЯ [Х] соблюдено [ ] не соблюдено. Пояснения: см. Примечания 3. ФОРМУЛА ИЗОБРЕТЕНИЯ: [Х] приняты во внимание все пункты (см. Примечания) [ ] приняты во внимание следующие пункты: [ ] принята во внимание измененная формула изобретения (см. Примечания) 4. КЛАССИФИКАЦИЯ ОБЪЕКТА ИЗОБРЕТЕНИЯ (ПОЛЕЗНОЙ МОДЕЛИ) (Указываются индексы МПК и индикатор текущей версии) (070 487/04 (2006.01) Аб1К 31/5377 (2006.01) Аб1К 45/06 (2006.01) Аб1К 31/519 (2006.01) Аб1К 31/541 (2006.01) Аб1Р 7/04 (2006.01) 5. ОБЛАСТЬ ПОИСКА 5.1 Проверенный минимум документации РСТ (указывается индексами МПК) С07О 487/04, Аб1К 31/519, Аб1К 31/5377, Аб1К 31/541, Аб1К 45/06, Аб1Р 7/04 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): ЕАРАТГУ, Езрасепек, ]-Р]1а Ра, РАТЕМТЗСОРЕ, Рабеагсв ...

HERBIZIDWIRKSAME ZUSAMMENSETZUNG

Die Erfindung betrifft herbizidwirksame Zusammensetzungen. Ziel der Erfindung ist die Bereitstellung von Zusammensetzungen mit guter herbizider Wirkung, die fuer die selektive Unkrautbekaempfung in landwirtschaftlichen Kulturen geeignet sind. Erfindungsgemaess werden als Wirkstoff in den neuen Zusammensetzungen Pyrazolverbindungen mit der Strukturformel angewandt, worin beispielsweise bedeuten: R hoch 1 einen C tief 1- C tief 4-halogenalkylrest; R hoch 2 eine C tief 1- C tief 4-alkylgruppe, C tief 5- C tief 6-cycloalkylgruppe, C tief 7- C tief 9-aralkylgruppe, C tief 7- C tief 9-alkarylgruppe, Phenyl- oder Naphthylrest oder eine5- oder 6gliedrige heterozyklische Gruppe mit Sauerstoff, Schwefel oder Stickstoff u.a.; R hoch 3 eine C tief 1- C tief 4-Alkylgruppe, eine C tief 2- C tief 4-alkenylgruppe, eine C tief 3- C tief 4-alkynylgruppe, eine C tief 2- C tief 6-alkoxyalkylgruppe oder eine C tief 2- C tief 6-alkylthioalkyruppe; R hoch 4 Wasserstoff, C tief 1- C tief 4-alkylgruppe oder eine Trihalogenmethylgruppe.

5-(INDOL-3-YLMETHYLENE)-1,3-DIMETHYL-2-METHYLIMINO-4-IMIDAZOLIDINONE

MEANS FOR COLORING KERATINFASERN CONTAINING A DIAMINE ON, N-DIHYDROPYRAZOLONDERIVAT, A KUPPLER AND A POLYOLE

Arylsulfonyl pyrazoline carboxamidine derivatives as 5-HT6 antagonists

This invention concerns arylsulfonyl pyrazoline carboxamidine derivatives as antagonists of 5- HT ...

PIPERIDINYLPYRAZOLOPYRIMIDINONES AND THEIR USE

The present application relates to novel substituted piperidinylpyrazolopyrimidinones, to processes for their preparation, the compounds for use alone or in combinations in a method for the treatment and/or prophylaxis of diseases, in particular for the treatment and/or prophylaxis of acute and recurrent bleeding in patients with or without underlying hereditary or acquired hemostatic disorders, wherein the bleeding is associated with a disease or medical intervention selected from the group consisting of heavy menstrual bleeding, postpartum hemorrhage, hemorrhagic shock, hemorrhagic cystitis, gastrointestinal hemorrhage, trauma, surgery, transplantation, stroke, liver diseases, hereditary angioedema, nosebleed, and synovitis and cartilage damage following hemarthrosis.

SUBSTITUTED BENZAMIDES FOR THE TREATMENT OF ARTHROPODS

The invention relates, inter alia, to compounds of general formula (I), where the groups A1-A4, T, n, W, Q, R1 and B1-B4 have the meanings indicated in the description. Also described are methods for producing the compounds of formula (I). The compounds of the invention are particularly suitable for controlling insects, arachnids and nematodes in agriculture and ectoparasites in veterinary medicine.

INDAZOLE DERIVATIVES AND THEIR USE AS INHIBITORS OF PHOSPHODIESTERASE (PDE) TYPE IV AND THE PRODUCTION OF TUMOR NECROSIS FACTOR (TNF)

The invention relates to compounds of formula (I) and pharmaceutically acceptable salts thereof, wherein R, R1, and R2, are as defined herein. The invention further relates to pharmaceutical compositions containing, and methods of using, the compounds of formula (I), or acceptable salts thereof, for the inhibition of phosphodiesterase (PDE) type IV or the production of tumor necrosis factor (TNF) in a mammal. The invention also relates to intermediates that are useful in the preparation of the compounds of formula (I).

SUBSTITUTED BENZAMIDES FOR TREATING ARTHROPODES

Substituted benzamides for the treatment of arthropods

SUBSTITUTED ARYLPYRAZOLES AS PARASITICIDAL AGENTS

ЗАМЕЩЕННЫЕ БЕНЗАМИДЫ ДЛЯ БОРЬБЫ С ЧЛЕНИСТОНОГИМИ

FIELD: chemistry.SUBSTANCE: invention relates to a compound of formula (I-T3), in which Ris C-C-alkyl; group: Ais C-H, Arepresents CRor N, Arepresents CR, Ais C-H, Brepresents CR, Bis C-H, Bis C-H and Brepresents CR, R, R, Rand Rindependently of each other are H, halogen, in each case optionally substituted with halogen C-C-alkyl, optionally substituted with halogen C-C-cycloalkyl or optionally substituted with halogen C-C-alkoxy; Ris a fluorine-substituted C-C-alkyl; Ris H; W is O; Q is cyclopropyl or 1-(cyano)-cyclopropyl.EFFECT: disclosed compounds are intended for use as an insecticide.4 cl, 6 tbl, 6 ex РОССИЙСКАЯ ФЕДЕРАЦИЯ (19) RU (11) (13) 2 712 092 C2 (51) МПК C07D 231/12 (2006.01) C07D 261/08 (2006.01) C07D 401/04 (2006.01) C07D 403/04 (2006.01) C07D 207/337 (2006.01) A01N 43/56 (2006.01) ФЕДЕРАЛЬНАЯ СЛУЖБА A01N 43/72 (2006.01) ПО ИНТЕЛЛЕКТУАЛЬНОЙ СОБСТВЕННОСТИ A01N 43/80 (2006.01) A01P 7/04 (2006.01) (12) ОПИСАНИЕ ИЗОБРЕТЕНИЯ К ПАТЕНТУ (52) СПК C07D 231/12 (2019.08); C07D 261/08 (2019.08); C07D 401/04 (2019.08); C07D 403/04 (2019.08); C07D 207/337 (2019.08); A01N 43/56 (2019.08); A01N 43/72 (2019.08); A01N 43/80 (2019.08) (24) Дата начала отсчета срока действия патента: 05.11.2014 Дата регистрации: Приоритет(ы): (30) Конвенционный приоритет: 05.11.2013 EP 13191610.8; 15.08.2014 EP 14181149.7 (43) Дата публикации заявки: 11.12.2017 Бюл. № 35 (73) Патентообладатель(и): БАЙЕР КРОПСАЙЕНС АКЦИЕНГЕЗЕЛЬШАФТ (DE) (85) Дата начала рассмотрения заявки PCT на национальной фазе: 06.06.2016 (86) Заявка PCT: R U 2 7 1 2 0 9 2 EP 2014/073794 (05.11.2014) (87) Публикация заявки PCT: WO 2015/067646 (14.05.2015) Адрес для переписки: 105064, Москва, а/я 88, "Патентные поверенные Квашнин, Сапельников и партнеры" (56) Список документов, цитированных в отчете о поиске: US 2011/0190365 A1, 04.08.2011. WO 2008/002671 A2, 03.01.2008. WO 03/087061 A1, 23.10.2003. US 2010/179141 A1, 15.07.2010. US 2010/286135 A1, 11.11.2010. RU 2474580 C2, 10.02.2013. WO 2011/009484 A1, 27.01.2011. ...

ЗАМЕЩЕННЫЕ БЕНЗАМИДЫ ДЛЯ БОРЬБЫ С ЧЛЕНИСТОНОГИМИ

FIELD: physics. SUBSTANCE: invention relates to compounds of formula (I-T3), in which R 1 is H, A 1 is C-H, A 2 represents CR 3 or N, A 3 represents CR 4 , A 4 is C-H, B 1 represents CR 6 or N, B 2 is C-H, B 4 is C-H and B 5 represents CR 10 or N, wherein substituents B 1 and B 5 do not simultaneously mean N, R 3 , R 4 , R 6 and R 10 independently of each other are H, halogen, cyano, nitro, in each case optionally substituted with halogen C 1 -C 6 -alkyl, optionally substituted with halogen C 3 -C 6 -cycloalkyl, optionally substituted with halogen C 1 -C 6 -alkoxy, optionally substituted with halogen C 1 -C 6 -alkylsulfanyl, optionally substituted with halogen C 1 -C 6 -alkylsulfinyl, optionally substituted with halogen C 1 -C 6 -alkylsulfonyl, optionally substituted with halogen N-C 1 -C 6 -alkylamino, optionally substituted with halogen N-C 1 -C 3 -alkoxy-C 1 -C 4 -alkylamino or optionally substituted with halogen 1-pyrrolidinyl; R 8 is a fluorine-substituted C 1 -C 4 -alkoxy or fluorine-substituted C 1 -C 4 -alkyl; R 11 is H; W is O or S; Q is C 1 -C 3 -alkyl, cyclopropyl, 1-(cyano)-cyclopropyl, 1-(perfluorinated C 1 -C 3 -alkyl)-cyclopropyl, 1-(C 1 -C 4 -alkyl)-cyclopropyl, 1-(thiocarbamoyl)-cyclopropyl, substituted with halogen C 1 -C 3 -alkyl, thiethane-3-yl, N-methyl-pyrazol-3-yl or 2-oxo-2 (2,2,2-trifluoroethylamino) ethyl. EFFECT: disclosed compounds are intended as an insecticide. 4 cl, 6 tbl, 6 ex РОССИЙСКАЯ ФЕДЕРАЦИЯ (19) RU (11) (13) 2 713 949 C2 (51) МПК C07D 231/12 (2006.01) C07D 261/08 (2006.01) C07D 401/04 (2006.01) C07D 403/04 (2006.01) C07D 207/337 (2006.01) A01N 43/56 (2006.01) ФЕДЕРАЛЬНАЯ СЛУЖБА A01N 43/72 (2006.01) ПО ИНТЕЛЛЕКТУАЛЬНОЙ СОБСТВЕННОСТИ A01N 43/80 (2006.01) A01P 7/04 (2006.01) (12) ОПИСАНИЕ ИЗОБРЕТЕНИЯ К ПАТЕНТУ (52) СПК C07D 231/12 (2019.08); C07D 261/08 (2019.08); C07D 401/04 (2019.08); C07D 403/04 (2019.08); C07D 207/337 (2019.08); A01N 43/56 (2019.08); A01N 43/72 (2019.08); A01N 43/80 (2019.08) 2016122093, 05.11.2014 (24) Дата ...

ПИРАЗОЛО[3,4-С]ПИРИДИНЫ И СПОСОБЫ ИХ ПРИМЕНЕНИЯ

FIELD: pharmacology. SUBSTANCE: subject of the invention is pyrazolo [3,4-c] pyridines of the formula I , including their stereoisomers, geometric isomers, tautomers and pharmaceutically acceptable salts, wherein R 1 and R 2 have the values disclosed in the claims. These compounds are useful for inhibiting Pim-kinases and for treating disorders such as cancer, mediated by Pim-kinase. Methods for using compounds of formula I for in vitro, in situ and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells or related pathological conditions are disclosed. EFFECT: increased application effeciency. 4 cl, 3 tbl, 328 ex

Светочувствительный полимерный материал с флуоресцентным считыванием информации, активируемый трихлорацетилпиразолином, и способ его получения

FIELD: optics. SUBSTANCE: invention relates to materials for optical recording of information, particularly materials for archival recording of information based on multilayer optical discs, with fluorescence reading. Light-sensitive polymer material with fluorescent information reading includes a precursor of a fluorescent compound of the lactone of Rhodamine B or Rhodamine 19 and a photo-generator of trichloroacetyl pyrazoline of general formula (1), dissolved in optically transparent polymer polymethyl methacrylate or polystyrene or copolymer of methyl methacrylate with ethyl acrylate. Also disclosed is a method of producing trichloracetyl pyrazoline by synthesis of 3-cynamoylcoumarine by condensation of 3-acetylcoumarin with ((4-formylphenyl)azanediyl)-di(ethane-2,1-diiyl)-diacetate followed by condensation of 3-cyano-miscumourin and phenylhydrazine to obtain pyrazolines, which are acylated with trichloroacetic acid chloride in methylene chloride in an ice bath in the presence of triethylamine. EFFECT: invention enables to obtain a coloured fluorescent form of a precursor of a fluorescent compound under the effect of radiation in the wavelength range of 250–500 nm without introducing additional components into the polymer material. 4 cl, 9 ex, 4 dwg РОССИЙСКАЯ ФЕДЕРАЦИЯ (19) RU (11) (13) 2 725 766 C1 (51) МПК C09K 11/06 (2006.01) C07D 231/00 (2006.01) ФЕДЕРАЛЬНАЯ СЛУЖБА ПО ИНТЕЛЛЕКТУАЛЬНОЙ СОБСТВЕННОСТИ (12) ОПИСАНИЕ ИЗОБРЕТЕНИЯ К ПАТЕНТУ (52) СПК C09K 11/06 (2020.02); C07D 231/00 (2020.02) (21)(22) Заявка: 2019119932, 26.06.2019 (24) Дата начала отсчета срока действия патента: Дата регистрации: 06.07.2020 (45) Опубликовано: 06.07.2020 Бюл. № 19 2 7 2 5 7 6 6 R U (56) Список документов, цитированных в отчете о поиске: Чепцов Д.А., Синтез и фотохимические превращения 3(дигидрогетарил)кумаринов, автореферат диссертации, Москва, 07.12.2018. RU 2478116 C2, 27.03.2013. US 6027855 A1, 22.02.2000. US 20030073031 A1, 17.04.2003. (54) Светочувствительный полимерный ...

PYRAZOLINE INSECTICIDES

1-ARYL-5-HYDRAZINO-PYRAZOLES

PYRAZOLINE DERIVATIVES

PYRAZOLES AS HUMAN NON-PANCREATIC SECRETORY PHOSPHOLIPASE A2 INHIBITORS

A class of novel pyrazoles is disclosed together with the use of such compounds for inhibiting sPLA2 mediated release of fatty acids for treatment of conditions such as septic shock.

Substituted benzamides for treating arthropodes

The invention relates inter alia to compounds of general formula (I), in which the groups A ...

Indazole derivatives and their use as inhibitors of phosphodiesterase (pde) type iv and the production of tumor necrosis factor (tnf)

PYRAZOLO[3,4-C]PYRIDINE COMPOUNDS AND METHODS OF USE

Pyrazolo[3,4-c]pyridine compounds of Formula I, including stereoisomers, geometric isomers, tautomers, and pharmaceutically acceptable salts thereof, wherein R1 and R2 are as defined herein, are useful for inhibiting Pim kinase, and for treating disorders such as cancer mediated by Pim kinase. Methods of using compounds of Formula I for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed.

COMPOSITION FOR DYEING KERATINIC FIBRES COMPRISING A DIAMINO-N,N-DIHYDRO-PYRAZOLONE DERIVATIVE, A COUPLING AGENT AND A POLYOL

ARYLOXIME LINKERS IN THE SOLID-PHASE SYNTHESIS OF 3-AMINOBENZISOXAZOLES

Dans une première variante, l'invention porte sur un procédé, induit par un support solide, de synthèse de divers hétérocycles polycycliques selon la formule générale (V). Dans une deuxième variante, l'invention porte sur un composé intermédiaire lié à un support solide qui peut être éventuellement dérivatisé avant qu'une procédure de cyclisation et de déplacement génère un produit. L'intermédiaire est de préférence stable par rapport à une large plage de conditions chimiques, ce qui permet, si souhaité, la dérivatisation chimique de l'intermédiaire. Dans un troisième aspect, l'invention porte sur une bibliothèque de divers composés qui contient une pluralité de composés divers de la formule générale (V). Dans un quatrième variante, l'invention porte sur un procédé de synthèse d'une bibliothèque de divers hétérocycles polycycliques. Dans une cinquième variante, l'invention porte sur un kit de dosage utilisé dans l'identification de composés de plomb de la bibliothèque précitée.

Patent RU2016122093A3

`”ВУ“” 2016122093” АЗ Дата публикации: 31.07.2018 Форма № 18 ИЗ,ПМ-2011 Федеральная служба по интеллектуальной собственности Федеральное государственное бюджетное учреждение 5 «Федеральный институт промышленной собственности» (ФИПС) ОТЧЕТ О ПОИСКЕ 1. . ИДЕНТИФИКАЦИЯ ЗАЯВКИ Регистрационный номер Дата подачи 2016122093/04(034556) 05.11.2014 РСТ/ЕР2014/073795 05.11.2014 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. 13191610.8 05.11.2013 ЕР 2. 14181149.7 15.08.2014 ЕР Название изобретения (полезной модели): [Х] - как заявлено; [ ] - уточненное (см. Примечания) ЗАМЕЩЕННЫЕ БЕНЗАМИДЫ ДЛЯ БОРЬБЫ С ЧЛЕНИСТОНОГИМИ Заявитель: БАЙЕР КРОПСАЙЕНС АКЦИЕНГЕЗЕЛЬШАФУТ, ОЕ 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: р [ ] принята во внимание измененная формула изобретения (см. Примечания) 4. КЛАССИФИКАЦИЯ ОБЪЕКТА ИЗОБРЕТЕНИЯ (ПОЛЕЗНОЙ МОДЕЛИ) (Указываются индексы МПК и индикатор текущей версии) (070 231/12 (2006.01) (070 403/04 (2006.01) АО1М 43/72 (2006.01) (070 261/08 (2006.01) (070 207/337 (2006.01) АО1М 43/80 (2006.01) (070 401/04 (2006.01) АО01М 43/56 (2006.01) АОГР 7/04 (2006.0Т) 5. ОБЛАСТЬ ПОИСКА 5.1 Проверенный минимум документации РСТ (указывается индексами МПК) С07О 231/12, С07О 261/08, СО7О 401/04, С07Р 403/04, СО7РО 207/337 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, ...

Patent RU2016122094A3

ЗАМЕЩЕННЫЕ БЕНЗАМИДЫ ДЛЯ БОРЬБЫ С ЧЛЕНИСТОНОГИМИ

1-ARYL-5-HYDRAZINO-PYRAZOLE

Substituted benzamides for the treatment of arthropods

The invention relates, inter alia, to compounds of general formula (I), where the groups A ...

PYRAZOLE DERIVATIVES, A PROCESS FOR THEIR PREPARATION AND THEIR USE AS HERBICIDES

Pyrazo1e derivatives of the formula in which X each independently is a halogen atom, and R is a halogen atom or an aryl group optionally substituted by halogen or C to C6 alkyl, which possess herbicidal activity.

SUBSTITUTED BENZAMIDES FOR TREATING ARTHROPODES

The invention relates inter alia to compounds of general formula (I), in which the groups A1-A4, T, n, W, Q, R1 and B1-B4 are defined as cited in the description. Further disclosed are methods for producing the compounds of formula (I). The compounds according to the invention are in particular suitable for controlling insects, arachnids and nematodes in agricultural applications and for controlling ectoparasites in veterinary medicine.

Arylsulfonyl pyrazoline carboxamidine derivatives as 5-HT6 antagonists

Novel compounds for controlling arthropods

本發明係關於尤其是通式(I)化合物 其中，A 1 -A 4 ，T，n，W，Q，R 1 及B 1 -B 4 基團各自係定義如說明書中。本文中亦說明者為製備式(I)化合物的方法。本發明化合物尤其適用於控制於農業上之昆蟲，蜘蛛及線蟲，以及於獸醫學之體外寄生蟲。

Arylsulfonyl pyrazoline carboxamidine derivatives as 5-HT6 antagonists

This invention concerns arylsulfonyl pyrazoline carboxamidine derivatives as antagonists of 5-ht6 receptors, to methods for the preparation of these compounds and to novel intermediates useful for their synthesis. The invention also relates to the uses of such compounds and compositions, particularly their use in administering them to patients to achieve a therapeutic effect in Parkinson's disease, Huntington's chorea, schizophrenia, anxiety, depression, manic depression, psychoses, epilepsy, obsessive compulsive disorders, mood disorders, migraine, Alzheimer's disease, age related cognitive decline, mild cognitive impairment, sleep disorders, eating disorders, anorexia, bulimia, binge eating disorders, panic attacks, akathisia, attention deficit hyperactivity disorder, attention deficit disorder, withdrawal from abuse of cocaine, ethanol, nicotine or benzodiazepines, pain, disorders associated with spinal trauma or head injury, hydrocephalus, functional bowel disorder, irritable bowel ...

ПИПЕРИДИНИЛПИРАЗОЛОПИРИМИДИНОНЫ И ИХ ПРИМЕНЕНИЕ

РОССИЙСКАЯ ФЕДЕРАЦИЯ (19) RU (11) (13) 2017 119 419 A (51) МПК C07D 487/04 (2006.01) ФЕДЕРАЛЬНАЯ СЛУЖБА ПО ИНТЕЛЛЕКТУАЛЬНОЙ СОБСТВЕННОСТИ (12) ЗАЯВКА НА ИЗОБРЕТЕНИЕ (21)(22) Заявка: 2017119419, 30.10.2015 (71) Заявитель(и): БАЙЕР ФАРМА АКЦИЕНГЕЗЕЛЬШАФТ (DE) Приоритет(ы): (30) Конвенционный приоритет: 03.11.2014 EP 14191410.1; 30.04.2015 EP 15165918.2 34 (85) Дата начала рассмотрения заявки PCT на национальной фазе: 05.06.2017 EP 2015/075208 (30.10.2015) (87) Публикация заявки PCT: R U Адрес для переписки: 105064, Москва, а/я 88, ООО "Патентные поверенные Квашнин, Сапельников и партнеры" (54) ПИПЕРИДИНИЛПИРАЗОЛОПИРИМИДИНОНЫ И ИХ ПРИМЕНЕНИЕ (57) Формула изобретения 1. Соединение формулы (I-A) , в которой R1 выбран из водорода и C1-C5 алкила; R2 выбран из водорода, C1-C4 алкила, C1-C6 циклоалкила, C1-C4 галоалкила, карбоксила, C1-C4 алкилового сложного эфира, C1-C4 алкокси- C1-C4 алкила, галогена, метилсульфанила, фенила, Стр.: 1 A 2 0 1 7 1 1 9 4 1 9 A WO 2016/071216 (12.05.2016) 2 0 1 7 1 1 9 4 1 9 (86) Заявка PCT: R U (43) Дата публикации заявки: 05.12.2018 Бюл. № (72) Автор(ы): ЭЛЛЕРМАНН Мануэль (DE), ФАЛОТ Гелле (DE), КАНХО ГРАНДЕ Иоланда (DE), ХАССФЕЛЬД Йорма (DE), КИНЦЕЛЬ Том (CN), КЁББЕРЛИНГ Йоханнес (DE), БАЙЕР Кристин (DE), РЁРИГ Зузанне (DE), ШПЕРЦЕЛЬ Михаэль (DE), ШТАМПФУСС Ян (DE), МАЙЕР Имке (DE), КЁЛЛЬНБЕРГЕР Мариа (DE), БУРКХАРДТ Нильс (DE), ШЛЕММЕР Карл-Хайнц (DE), ШТЕГМАНН Кристиан (DE), ШУМАХЕР Йоахим (DE), ВЕРНЕР Маттиас (DE), ХАЙЕРМАНН Йорг (DE), ХЕНГЕВЕЛЬД Виллем Ян (NL) 2 0 1 7 1 1 9 4 1 9 R U A Стр.: 2 2 0 1 7 1 1 9 4 1 9 R3 выбран из водорода, галогена, циано, C1-C4 алкила, причем алкил необязательно замещен ди- C1-C4 алкиламино, C1-C4 алкенила, C1-C4 алкилового сложного эфира, причем C1-C4 алкиловый сложный эфир необязательно замещен одним, двумя, тремя, четырьмя или пятью заместителями галоген, C3-C4 циклоалкилового сложного эфира, C3-C4 циклоалкила, карбоксила, карбоксамида, бензилового сложного эфира, -NH-COфенила, -CS-NH2, фенилсульфонила ...

ЗАМЕЩЕННЫЕ БЕНЗАМИДЫ ДЛЯ БОРЬБЫ С ЧЛЕНИСТОНОГИМИ

ИМИДАЗОЛИЕВЫЕ ЦВИТТЕР-ИОННЫЕ ПОЛИМЕРИЗУЕМЫЕ СОЕДИНЕНИЯ И СОДЕРЖАЩИЕ ИХ ОФТАЛЬМОЛОГИЧЕСКИЕ УСТРОЙСТВА

Группа изобретений относится к цвиттер-ионному полимеризуемому соединению формулы I где R1, R2 и R3 независимо представляют собой H, C1-C6 алкил; каждый из L1 и L2 независимо представляет собой C2-C6 алкилен; и Rg представляет собой (мет)акриламид, также относится к контактной линзе, содержащей полимер, полученный из цвиттер-ионного полимеризуемого соединения, где полимер содержит продукт свободнорадикальной реакции соединения и один или более мономеров, приемлемых для изготовления контактной линзы, где мономер выбран из гидрофильного компонента, также относится к блистерной упаковке, включающей в себя контактную линзу и упаковочный раствор, причем упаковочный раствор содержит полимер, полученный из полимеризуемого цвиттер-ионного соединения. Настоящие изобретения обеспечивает разработку новых цвиттер-ионных полимеризуемых соединений, которые приемлемы для применения в офтальмологических устройствах, таких как контактные линзы, офтальмологических устройств, которые показывают благоприятные ...

Substituted benzamides for treating arthropodes

The invention relates inter alia to compounds of general formula (I), in which the groups A ...

Arylsulfonyl pyrazoline carboxamidine derivatives as 5-HT antagonists

COMPOSED OF PIRAZOL, EQUIPMENT LIKE INHIBITORS OF the HALF-FULL LIBERATION OF ACIDS GREASY BY the FOSFOLIPASA HUMAN nonPANCREATIC SECRETORY A2, PROCEDURES TO PREPARE THESE COMPOUNDS AND FORMULATED PHARMACEUTICAL COMPOSITIONS WITH THESE COMPOUNDS

Se revela un tipo de compuestos de pirazol novedosos, y de aplicacion para inhibir la liberacion mediada por aPLA2 de ácidos grasos, en el tratamiento decondiciones tales como el shock séptico. Dichos compuestos tienen la formula (I): en dondeR1 es fenilo, isoquinolin-3-ilo, pirazinilo, piridin-2-ilo,piridin-2-ilo sustituido en posicion 4 con alquilo (C1-C4), alcoxilo (C1-C4), CH o -(CH2)nCONH2 donde n es 0-2; R2 es fenilo, fenilo sustituido con 1 a 3sustituyentes seleccionados entreel g rupo formado por alquilo (C1-C4), -CN, halo, -NO2, CO2 alquilo (C1-C4) y -CF3; naftilo, tiofeno o tiofeno sustituidocon 1 a 3 grupos halo; R3 es hidrogeno, fenilo, alquenilo (C2-C6) fenilo; piridilo, naftilo, quinolinilo,alquiltiazolilo (C1 -C4); fenilo sustituido con1 a 2 sustituyentes seleccionados a partir del grupo formado por alquilo (C1-C4), -CN, -CONH2, NO2, CF3, halo, alcoxi (C1-C4), CO2 alquilo (C1-C4),fenoxi y SR4 en donde R4, es alquilo (C1-C4) ohalofenilo; fenilo sus tituido con un sustituyente ...

ARYLSULFONYL PYRAZOLINE CARBOXAMIDINE DERIVATIVES AS 5-HT6 ANTAGONISTS

This invention concerns arylsulfonyl pyrazoline carboxamidine derivatives as antagonists of 5- HT6 receptors, to methods for the preparation of these compounds and to novel intermediates useful for their synthesis. The invention also relates to the uses of such compounds and compositions, particularly their use in administering them to patients to achieve a therapeutic effect in Parkinson's disease, Huntington's chorea, schizophrenia, anxiety, depression, manic depression, psychoses, epilepsy, obsessive compulsive disorders, mood disorders, migraine, Alzheimer's disease, age related cognitive decline, mild cognitive impairment, sleep disorders, eating disorders, anorexia, bulimia, binge eating disorders, panic attacks, akathisia, attention deficit hyperactivity disorder, attention deficit disorder, withdrawal from abuse of cocaine, ethanol, nicotine or benzodiazepines, pain, disorders associated with spinal trauma or head injury, hydrocephalus, functional bowel disorder, Irritable Bowel Syndrome, obesity and type-2 diabetes. The compounds have the general formula (1) wherein the symbols

5-(INDOL-3-YLMETHYLENE)-1,3-DIMETHYL-2-METHYLIMINO-4- IMIDAZOLIDINONE

ABSTRACT OF THE DISCLOSURE The invention relates to the novel 5-(indol-3--ylmethylene)-1,3-dimethyl-2-methylimino-4-imidazolidinone of the formula E-isomer or Z-isomer

Pirazóis como inibidores de fosfolipase a2 secretora não pancreática humana

Patente de Invenção: <B>"PIRAZóIS COMO INIBIDORES DE FOSFOLIPASE A~ 2~ SECRETORA NãO PANCREáTICA HUMANA"<D>. é revelada uma classe de novos pirazóis juntamente com a utilização de tais compostos para inibir liberação de ácidos graxos mediada por sPLA~ 2~, para tratamento de condições, tais como, choque séptico.

Nuevos compuestos para el combate de artrópodos.

SUBSTITUTED TRIAZOLYLMETHYLCARBINOLS

Arylsulfonyl pyrazoline carboxamidine derivatives as 5-HT6 antagonists

This invention concerns arylsulfonyl pyrazoline carboxamidine derivatives as antagonists of 5- HT ...

Pyrazoles as human non-pancreatic secretory phospholipase a₂ inhibitors

AROMATIC DERIVATIVE, PREPARATION METHOD FOR SAME, AND MEDICAL APPLICATIONS THEREOF

An aromatic derivative as represented by formula (I), a pharmaceutically acceptable salt thereof or a pharmaceutical composition comprising same, a preparation method therefor, and uses of the aromatic derivative and the pharmaceutically acceptable salt thereof or the pharmaceutical composition comprising same in preparing a therapeutic agent, specifically an FGFR4 tyrosine kinase inhibitor, and in preparing a medicament for treating and/or preventing neoplastic and inflammatory diseases. The substituents of formula (I) are same as defined in the description.

NOVEL COMPOUNDS FOR COMBATING ARTHROPODS

1,3-DIMETHYL-4- 2,4-DICHLOROBENZOYL -5-SUBSTITUTED- ACRYLOYLOXY PYRAZOLES

Aryloxime linkers in the solid-phase synthesis of 3-aminobenzisoxazoles

5-(INDOL-3-YLMETHYLENE)-1,3-DIMETHYL-2-METHYLIMINO-4- IMIDAZOLIDINONE

NOVEL COMPOUNDS FOR CONTROLLING ARTHROPODS

... in which the A1-A4, T, n, W, Q, R1 and B1-B4 radicals are each as defined in the description. Also described are processes for preparing the compounds of the formula (I). The inventive compounds are especially suitable for controlling insects, arachnids and nematodes in agriculture, and ectoparasites in veterinary medicine.

Pyrazole compound or salt thereof, and preparation method, herbicide composition and use thereof

Disclosed are a pyrazole compound or a salt thereof, and a preparation method, a herbicide composition and a use thereof. The pyrazole compound or salt thereof has the structure as shown in formula (I). In the formula (I), R represents , wherein R', R'' and R''' represent hydrogen atoms, C1-C4 alkyl, C1-C4 halogenated alkyl, C1-C4 alkyloxy or halogen, and may be the same or different; R1 represents a C1-C3 alkyl; R2 represents a hydrogen atom or C1-C4 alkyl; and R3 is a hydrogen atom or C1-C6 alkyl, a substitutable phenyl, a substitutable pyridyl, a substitutable alkenyl, a substitutable alkynyl, a C1-C6 alkylcarbonyl, a C1-C6 alkyloxycarbonyl, a C1-C6 alkylcarbonylmethyl and the like. The pyrazole structure not only shows an excellent herbicidal effect on barnyard grass, but is also safe to apply to rice after seedling emergence. More surprisingly, it also exerts an outstanding effect on barnyard grass with resistance to the main barnyard grass herbicides such as penoxsulam, quinclorac ...

Herbicidal substituted pyrazole-4-(thio) carboxylates

Novel pyrazoles have the formula wherein R<1> is C1-C4 haloalkyl or ROR<5>, wherein R is C1-C2 alkylene or C2 alkylidene and R<5> is hydrogen, C1-C4 alkyl, C2-C5 alkanoyl, aroyl, C8-C10 aralkanoyl, C7-C9 aralkyl, phenyl, or phenyl substituted with C1-C4 alkyl, C1-C4 alkoxy, trihalomethyl, hydroxy, cyano or nitro; or benzoyl substituted with halogen, C1-C4 alkyl, C1-C4 alkoxy, trihalomethyl hydroxy, cyano or nitro; R<2> is C1-C4 alkyl, C5-C6 cycloalkyl, C7-C9 aralkyl, C7-C9 alkaryl, phenyl, naphthyl or a 5- or 6-membered heterocyclic group containing oxygen, sulfur or nitrogen, or R2 is phenyl substituted with halogen, trihalomethyl, C1-C4 alkoxy, hydroxy or cyano; Y is oxygen or sulfur, R<3> is C1-C4 alkyl, C2-C4 alkenyl, C3-C4 alkynyl, C2-C8 alkoxyalkyl or C2-C6 alkylthioalkyl; R<4> is hydrogen, C1-C4 alkyl or trihalomethyl; provided that R<2> is not 3,4-dialkylphenyl or 3,4 dihalophenyl, and are used for the preemergence and post-emergence treatment of weeds.

SUBSTITUTED PYRAZOLE HERBICIDES

Substituted benzamides for treating arthropodes

The invention relates inter alia to compounds of general formula (I), in which the groups A ...

SUBSTITUTED TRIAZOLYLMETHYLCARBINOLS

Benzamidas sustituidas para tratamiento de artrópodos.

Substituted arylpyrazoles as parasiticidal agents

Piperidinylpyrazolopyrimidinones and their use

The present application relates to novel substituted piperidinylpyrazolopyrimidinones, to processes for their preparation, the compounds for use alone or in combinations in a method for the treatment and/or prophylaxis of diseases, in particular for the treatment and/or prophylaxis of acute and recurrent bleeding in patients with or without underlying hereditary or acquired hemostatic disorders, wherein the bleeding is associated with a disease or medical intervention selected from the group consisting of heavy menstrual bleeding, postpartum hemorrhage, hemorrhagic shock, hemorrhagic cystitis, gastrointestinal hemorrhage, trauma, surgery, transplantation, stroke, liver diseases, hereditary angioedema, nosebleed, and synovitis and cartilage damage following hemarthrosis.

PYRAZOLINE DERIVATIVES

Pyrazole compound or a salt thereof, preparation method, herbicide composition and use thereof

Piperidinylpyrazolopyrimidinones and their use

The present application relates to novel substituted piperidinylpyrazolopyrimidinones, to processes for their preparation, the compounds for use alone or in combinations in a method for the treatment and/or prophylaxis of diseases, in particular for the treatment and/or prophylaxis of acute and recurrent bleeding in patients with or without underlying hereditary or acquired hemostatic disorders, wherein the bleeding is associated with a disease or medical intervention selected from the group consisting of heavy menstrual bleeding, postpartum hemorrhage, hemorrhagic shock, hemorrhagic cystitis, gastrointestinal hemorrhage, trauma, surgery, transplantation, stroke, liver diseases, hereditary angioedema, nosebleed, and synovitis and cartilage damage following hemarthrosis.

Indazole derivatives and their use as inhibitors of phosphodiesterase (PDE) type IV and the production of tumor necrosis factor (TNF)

Substituted benzamides for the treatment of arthropods

The invention relates, inter alia, to compounds of general formula (I), where the groups A ...

Arylsulfonyl pyrazoline carboxamidine derivatives as 5-HT antagonists

SUBSTITUIERTE TRIAZOLYLMETHYLCARBINOLE

Substituted arylpyrazoles as parasiticidal agents

INDAZOLE DERIVATIVES, PHARMACEUTICAL COMPOSITIONS AND APPLICATION THEREOF

The invention relates to compounds with the formula to their pharmaceutically acceptable salts and the intermediate compounds for their preparation. In the formula radicals R, R1 & R2 have the meanings listed in the description. The invention also relates to pharmaceutical compositions which contain the above compounds and to methods for the usage of the compounds or their acceptable salts for the inhibition of the phosphodiesterase (PDE) type IV or the production of tumournectrotic factor (TNF) in mammals.

REPLACED ARILPIRAZOLES, A PROCEDURE FOR ITS PREPARATION, PHARMACEUTICAL OR VETERINARY COMPOSITIONS CONTAIN THAT THEM AS ACTIVE PRINCIPLE AND ITS USE IN THE MANUFACTURE OF A HUMAN MEDICINE PARASITICIDA OR ANIMAL.

Un compuesto de 1-aril-4-ciclopropilpirazoles en los que al menos un fluor está unido al anillo de ciclopropilo, a composiciones que comprenden tales compuestos, a procedimientos para su síntesis y a su uso como parasiticidas. Reivindicacion 1: Un compuesto de formula (1), en la que: R1 es CF3, OCF2H, OCF3, -SCF3, -SOCF3, -SO2CF3 o SF5; R2 es H, fluoro o alquilo C1-4 opcionalmente sustituido con de 1 a 5 átomos de halogeno seleccionados independientemente entre cloro y fluoro; R3, R4, R5 y R6 representan independientemente H, alquilo C1-4 opcionalmente sustituido con de 1 a 5 grupos de halogeno seleccionados independientemente entre cloro y fluoro, o un cloro o fluoro; R7 es Cl o fluoro; X es CR8 o N donde R8 es Cl o fluoro; y R9 es NRaRb; Ra se selecciona entre hidrogeno, alquilo C1-6, alquenilo C2-6, cicloalquilo C3-8, C(O)O-alquilo(C1-6) y alcanoilo C1-6, donde cada uno de los grupos anteriores puede incluir uno o más sustituyentes opcionales donde sea químicamente posible seleccionados independientemente entre halo, het, fenilo, hidroxi, -C(O)OH, -C(O)O-alquilo(C1-6), alquilo C1-6, haloalquilo C1-6, cicloalquilo C3-8, alcoxi C1-6, haloalcoxi C1-6, amino, alquil(C1-6)-amino y di-alquil(C1-6)-amino; Rb se selecciona entre hidrogeno, alquilo C1-6, alquenilo C2-6, alcanoilo C1-6 y C(O)O-alquilo(C1-6), donde cada uno de los grupos anteriores puede incluir uno o más sustituyentes opcionales donde sea químicamente posible seleccionados independientemente entre halo, fenilo, hidroxi, -COOH, -C(O)O-alquilo(C1-6), alquilo C1-6, haloalquilo C1-6, cicloalquilo C3-8, alcoxi C1-6, haloalcoxi C1-6, amino, alquil(C1-6)-amino y di-alquil(C1-6)-amino; o Ra y Rb junto con el átomo N al que están unidos pueden formar un anillo heterocíclico de tres a siete miembros que contiene uno o más átomos N, O o S adicionales y donde dicho anillo heterocíclico puede tener uno o más sustituyentes opcionales seleccionados entre el grupo compuesto por oxo, halo, het, fenilo, hidroxi, -COOH, -C(O ...

Pyrazole als humane nicht-pankreatische sekretorische Phospholipase-A2-Inhibitoren

Strobilurin Type Compounds for Combating Phytopathogenic Fungi

The present invention relates to novel strobilurine type compounds, to compositions comprising at least one such compound, to methods for combating phytopathogenic fungi, to the use of such compounds and to seeds coated with at least one such compound.

PYRAZOLE DERIVATIVE AND USE THEREOF

Provided is a novel PDGFR kinase inhibitor, comprising a compound of formula (I) or a pharmaceutically acceptable salt, solvate, ester, acid, metabolite or prodrug thereof. Further provided are use and a method of the compound of formula (I) for preventing or treating conditions associated with PDGFR kinase activity, particularly use and a method for preventing or treating conditions associated with PDGFRα and/or PDGFRβ kinase activity.

Novel compounds for controlling arthropods

The invention relates inter alia to compounds of the general formula (I)in which the A1-A4, T, n, W, Q, R1 and B1-B4 radicals are each as defined in the description. Also described are processes for preparing the compounds of the formula (I). The inventive compounds are especially suitable for controlling insects, arachnids and nematodes in agriculture, and ectoparasites in veterinary medicine.

FOR THE TREATMENT OF SUBSTITUTED BENZAMIDES ARTHROPOD

LA INVENCIÓN SE REFIERE INTER ALIA A COMPUESTOS DE LA FÓRMULA GENERAL (I): (VER FORMULA); EN DONDE LOS RADICALES A1-A4, T, N, W, Q, R1 Y B1-B4 SON CADA UNO COMO SE DEFINE EN LA DESCRIPCIÓN. TAMBIÉN SE DESCRIBEN PROCESOS PARA PREPARAR LOS COMPUESTOS DE LA FÓRMULA (I). LOS COMPUESTOS DE LA INVENCIÓN SON EN ESPECIAL APROPIADOS PARA CONTROLAR INSECTOS, ARÁCNIDOS Y NEMATODOS EN AGRICULTURA Y ECTOPARÁSITOS EN MEDICINA VETERINARIA

5-(Indol-3-ylmethylene)-1,3-dimethyl-2-methylamino-4-imidazolidinone

... 5-(Indol-3-ylmethylene)-1,3-dimethyl-2-methylimino-4-imidazolidinone and its geometric isomers, prepared, inter alia, from indole-3-aldehyde and 1,3-dimethyl-2-methylimino-4-imidazolidinone, are described. The end products are useful as antidepressants.

Pyrazole derivatives as inhibitors of STAT3

Compositions that modulate the activity of signal transducer and activator of transcription-3 (STAT3) activity as well as their methods of use, such as treatment and imaging are provided. Compositions contain small molecules such as substituted pyrazoles and are useful in treatment of diseases related to the activity of STAT3 including, for example, cancer and other diseases.

Strobilurin type compounds for combating phytopathogenic fungi

本发明涉及新型嗜球果伞素类型化合物、包含至少一种该类化合物的组合物、防治植物病原性真菌的方法、该类化合物的用途以及涂有至少一种该类化合物的种子。

절지동물 방제용 치환 벤즈아미드

... 본 발명은 특히 화학식 (I)의 화합물에 관한 것이다: 상기 식에서, A1-A4, T, n, W, Q, R1 및 B1-B4 래디칼은 각각 명세서에 정의된 바와 같다. 또한 본 발명은 화학식 (I)의 화합물의 제조방법에 관한 것이다. 본 발명의 화합물은 농업에서 곤충, 거미류 및 선충을, 수의약으로 외부기생충을 방제하는데 특히 적합하다.

PYRAZOLE DERIVATIVES AS INHIBITORS OF STAT3

Compositions that modulate the activity of signal transducer and activator of transcription-3 (STAT3) activity as well as their methods of use, such as treatment and imaging are provided. Compositions contain small molecules such as substituted pyrazoles and are useful in treatment of diseases related to the activity of STAT3 including, for example, cancer and other diseases.

Substituted arylpyrazoles

This invention relates to a range of 1-aryl-4-cyclopropylpyrazoles in which there is at least one fluorine attached to the cyclopropyl ring, to compositions comprising such compounds, processes to their synthesis and their use as parasiticides.

Mittel zum Färben von Keratinfasern enthaltend ein Diamino-N,N-Dihydropyrazolonderivat, einen Kuppler und ein Polyol

1-ARYL-5-HYDRAZINO-PYRAZOLE

Treating diabetes with dipeptidyl peptidase-IV inhibitors

The present invention is directed to novel substituted dihydropyrrolopyrazoles of structural Formula I which are inhibitors of the dipeptidyl peptidase-N enzyme and which are useful in the treatment or prevention of diseases in which the dipeptidyl peptidase-IV enzyme is involved, such as diabetes and particularly Type 2 diabetes. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which the dipeptidyl peptidase IV enzyme is involved.

Pyrazole als humane nicht-pankreatische sekretorische Phospholipase-A2-Inhibitoren

PYRAZOLO[3,4-c]PYRIDINE COMPOUNDS AND METHODS OF USE

Pyrazolo[3,4-c]pyridine compounds of Formula I, including stereoisomers, geometric isomers, tautomers, and pharmaceutically acceptable salts thereof, wherein R 1 and R 2 are as defined herein, are useful for inhibiting Pim kinase, and for treating disorders such as cancer mediated by Pim kinase. Methods of using compounds of Formula I for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed.

ARYLSULFONYL PYRAZOLINE CARBOXAMIDINE DERIVATIVES AS 5-HT6 ANTAGONISTS

This invention concerns arylsulfonyl pyrazoline carboxamidine derivatives as antagonists of 5-ht6 receptors, to methods for the preparation of these compounds and to novel intermediates useful for their synthesis. The invention also relates to the uses of such compounds and compositions, particularly their use in administering them to patients to achieve a therapeutic effect in Parkinson's disease, Huntington's chorea, schizophrenia, anxiety, depression, manic depression, psychoses, epilepsy, obsessive compulsive disorders, mood disorders, migraine, Alzheimer's disease, age related cognitive decline, mild cognitive impairment, sleep disorders, eating disorders, anorexia, bulimia, binge eating disorders, panic attacks, akathisia, attention deficit hyperactivity disorder, attention deficit disorder, withdrawal from abuse of cocaine, ethanol, nicotine or benzodiazepines, pain, disorders associated with spinal trauma or head injury, hydrocephalus, functional bowel disorder, irritable bowel syndrome, obesity and type-2 diabetes. The compounds have the general formula (1) wherein the symbols have the meanings given in the description. 18-. (canceled)16. The method of claim 11 , wherein the compound is an optically active enantiomer.17. The method of claim 11 , further comprising at least one additional therapeutic agent. This invention relates to the fields of pharmaceutical and organic chemistry, and provides arylsulfonyl pyrazoline carboxamidine derivatives, intermediates, formulations and methods.Serotonin (5-hydroxytryptamine or 5-HT), a key transmitter of the peripheral and central nervous system, modulates a wide range of physiological and pathological functions, mediated through a number of receptor families termed 5-HT, 5-HT, 5-HT, 5-HT, 5-HT, 5-HTand 5-HT. Although the functions of the latter three are less well understood than those of the others, it is generally accepted that compounds which selectively interfere with 5-HT-mediated signal transduction are ...

Piperidinylpyrazolopyrimidinones and their use

The present application relates to novel substituted piperidinylpyrazolopyrimidinones, to processes for their preparation, the compounds for use alone or in combinations in a method for the treatment and/or prophylaxis of diseases, in particular for the treatment and/or prophylaxis of acute and recurrent bleeding in patients with or without underlying hereditary or acquired hemostatic disorders, wherein the bleeding is associated with a disease or medical intervention selected from the group consisting of heavy menstrual bleeding, postpartum hemorrhage, hemorrhagic shock, hemorrhagic cystitis, gastrointestinal hemorrhage, trauma, surgery, transplantation, stroke, liver diseases, hereditary angioedema, nosebleed, and synovitis and cartilage damage following hemarthrosis.

Method of controlling weeds

Изобретение относитс  к области химических способов борьбы с сорной и нежелательной растительностью. С целью усилени  гербицидного действи  обработку растений или почвы осуществл ют производными пиразола общей формулы N CH-C(CN)C(NHa)-N(Ar), где Аг - 2-хлор-4-трифторметилфенил, 2,6-дихлор-4-трифторметилфенил, 2,3, 6-трихлор-4-трифторметилфенил, 2,3, 5,6-тетрафтор :4-трифторметилфенил. При дозах активных веществ 0,0156- -1 кг/га способ эффективен дл  избирательной борьбы с сорн ками в посевах культурных растений, например пшеницы. 2 табл. ОТ This invention relates to the field of chemical methods for controlling weeds and unwanted vegetation. In order to enhance the herbicidal effect, the treatment of plants or soil is carried out by pyrazole derivatives of the general formula N CH-C (CN) C (NHa) -N (Ar), where Ar is 2-chloro-4-trifluoromethylphenyl, 2,6-dichloro-4 trifluoromethylphenyl, 2,3, 6-trichloro-4-trifluoromethylphenyl, 2,3, 5,6-tetrafluoro: 4-trifluoromethylphenyl. With doses of active substances of 0.0156-1 kg / ha, the method is effective for selectively controlling weeds in crops of cultivated plants, such as wheat. 2 tab. FROM

Indazole derivatives and their use as inhibitors of phosphodiesterase (pde) type iv and the production of tumor necrosis factor (tnf)

The invention relates to compounds of formula (I) and pharmaceutically acceptable salts thereof, wherein R, R1, and R2, are as defined herein. The invention further relates to pharmaceutical compositions containing, and methods of using, the compounds of formula (I), or acceptable salts thereof, for the inhibition of phosphodiesterase (PDE) type IV or the production of tumor necrosis factor (TNF) in a mammal. The invention also relates to intermediates that are useful in the preparation of the compounds of formula (I).

Herbicidni prostredek

Indazole Derivatives and Their Use as Inhibitors of Phosphodiesterase (PDE) type IV and the Production of Tumor Necrosis Factor (TNF)

(여기서, R, R 1 및 R 2 는 상기 정의된 바와 같음) Wherein R, R 1 and R 2 are as defined above 본 발명은 화학식 I의 화합물 및 제약학적으로 허용 가능한 그의 염이다. 또한, 본 발명은 포유동물에서 포스포디에스터라제 (PDE) 유형 IV 또는 종양 괴사 인자 (TNF) 생산의 억제를 위한, 화학식 I의 화합물 또는 제약학적으로 허용 가능한 그의 염을 포함하는 조성물, 및 그의 사용 방법에 관한 것이다. 또한, 본 발명은 화학식 I의 화합물의 제조에 유용한 중간체에 관한 것이다. The present invention is a compound of formula (I) and a pharmaceutically acceptable salt thereof. The invention also provides a composition comprising a compound of formula (I) or a pharmaceutically acceptable salt thereof, for the inhibition of phosphodiesterase (PDE) type IV or tumor necrosis factor (TNF) production in a mammal, and It is about how to use. The present invention also relates to intermediates useful for the preparation of compounds of formula (I).

Novel compounds for combating arthropods

Substituted arylpyrazoles as parasiticidal agents

This invention relates to a range of 1-aryl-4-cyclopropylpyrazoles in which there is at least one fluorine attached to the cyclopropyl ring, to compositions comprising such compounds, processes to their synthesis and their use as parasticides.

N-phenylpyrazole 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。

Piperidinylpyrazolopyrimidinones and their use

The present application relates to novel substituted piperidinylpyrazolopyrimidinones, to processes for their preparation, the compounds for use alone or in combinations in a method for the treatment and/or prophylaxis of diseases, in particular for the treatment and/or prophylaxis of acute and recurrent bleeding in patients with or without underlying hereditary or acquired hemostatic disorders, wherein the bleeding is associated with a disease or medical intervention selected from the group consisting of heavy menstrual bleeding, postpartum hemorrhage, hemorrhagic shock, hemorrhagic cystitis, gastrointestinal hemorrhage, trauma, surgery, transplantation, stroke, liver diseases, hereditary angioedema, nosebleed, and synovitis and cartilage damage following hemarthrosis.

SUBSTITUTED ARYLPYRAZOLES AS PARASITICIDES

La présente invention concerne une gamme de 1-aryl-4-cyclopropylpyrazoles dans lesquels il existe au moins un atome de fluor fixé au noyau cyclopropyle, des compositions comprenant ces composés, des procédés pour leur synthèse ainsi que leur utilisation comme parasiticides.

Non-systemic TGR5 agonists

The present invention relates to sulfonamide compounds of formula (I) and formula (II), or a pharmaceutically acceptable salt thereof. The present sulfonamide compounds are useful non-systemic TGR5 agonists that can be used to treat diabetic diseases in human. The present invention provides a pharmaceutical composition containing sulfonamide compounds of formula (I) and formula (II) and a method of making as well as a method of using same in treating patients inflicted with metabolic disorders by administering same. The compounds of the present invention may be used in combination with additional anti-diabetic drugs.

Pyrazoline insecticides

Novel compounds for combating arthropods

Pyrazoline derivatives and insecticidal compositions

5-(indol-3-ylmethylene)-1,3-dimethyl-2-methylimino-4-imidazolynone

Compounds for controlling arthropods

The invention relates inter alia to compounds of the general formula (I) in which the A 1 -A 4 , T, n, W, Q, R 1 and B 1 -B 4 radicals are each as defined in the description. Also described are processes for preparing the compounds of the formula (I). The inventive compounds are especially suitable for controlling insects, arachnids and nematodes in agriculture, and ectoparasites in veterinary medicine.

Substituted benzamides for treating arthropods

Crystalline forms of a tlr7/tlr8 inhibitor

本申請涉及處於其游離形式的( S) - N -(4-((5-(1,6-二甲基-1 H -吡唑并[3,4-b]吡啶-4-基)-3-甲基-4,5,6,7-四氫-1 H -吡唑并[4,3-c]吡啶-1-基)甲基)雙環[2.2.2]辛烷-1-基) 啉-3-甲醯胺的不同晶型，連同組成物、其製備方法、以及其使用方法。在一些實施方式中，晶型也含有水(“水合物”)。該等材料在不同自身免疫性疾病的治療中是有用的，該等自身免疫性疾病包括全身性紅斑狼瘡、皮膚狼瘡、盤狀狼瘡、混合性結締組織病、原發性膽汁性肝硬化、免疫性血小板減少性紫癜、化膿性汗腺炎、皮肌炎、多發性肌炎、乾燥綜合征、關節炎、類風濕關節炎和銀屑病。

SUBSTITUTED ARYLPYRAZOLE AS PARASITICIDES

Pyrazole derivatives as inhibitors of stat3

Compositions that modulate the activity of signal transducer and activator of transcription-3 (STAT3) activity as well as their methods of use, such as treatment and imaging are provided. Compositions contain small molecules such as substituted pyrazoles and are useful in treatment of diseases related to the activity of STAT3 including, for example, cancer and other diseases.

PIPERIDINILPIRAZOLOPIRIMIDINONAS AND USE OF THE SAME

La presente solicitud de patente se refiere a novedosas piperidinilpirazolopirimidinonas sustituidas, a los procesos para la preparación de las mismas, a los compuestos que pueden utilizarse en forma aislada o combinada en un método para el tratamiento y/o la profilaxis de enfermedades, en particular para el tratamiento y/o la profilaxis de sangrado agudo y recurrente en pacientes con o sin trastornos hemostáticos hereditarios o adquiridos subyacentes, donde el sangrado está asociado con una enfermedad o intervención médica a seleccionar a partir del conjunto que consiste en sangrado menstrual abundante, hemorragia post parto, shock hemorrágico, cistitis hemorrágicas, hemorragia gastrointestinal, etc.

PIRAZOLINE DERIVATIVES

Substituted benzamides for treating arthropodes

The invention relates inter alia to compounds of general formula (I), in which the groups A1-A4, T, n, W, Q, R1 and B1-B4 radicals are each as defined in the description. Also described are processes for preparing the compounds of formula (I). The inventive compounds are especially suitable for controlling insects, arachnids and nematodes in agriculture, and ectoparasites in veterinary medicine.

Arylsulfonylpyrazolincarboxamidinderivater as 5-ht6 antagonists

ARYLSULPHONYLPYRAZOLINCARBOXAMIDINE DERIVATIVES AS ANTAGONISTS OF 5-NT

Настоящее изобретение относится к арилсульфонилпиразолинкарбоксамидиновым производным в качестве антагонистов рецепторов 5-HT, к способам получения этих соединений и к новым промежуточным соединениям, применимым в их синтезе. Кроме того, настоящее изобретение относится к применениям указанных соединений и композиций, в частности их применению для введения пациентам с целью достижения терапевтического эффекта при лечении болезни Паркинсона, хореи Хантингтона, шизофрении, тревожности, депрессии, маниакально-депрессивного психоза, психозов, эпилепсии, обсессивно-компульсивных расстройств, аффективных расстройств, мигрени, болезни Альцгеймера, возрастного ослабления когнитивных способностей, умеренных когнитивных нарушений, расстройств сна, расстройств, связанных с питанием, анорексии, булимии, расстройств, связанных с перееданием, приступов панического расстройства, акатизии, синдрома дефицита внимания и гиперактивности, синдрома дефицита внимания, избавления от пагубных пристрастий к кокаину, этанолу, никотину или бензодиазепинам, боли, расстройств, связанных с травмами позвоночника и/или поражениями головы, гидроцефалии, расстройств деятельности кишечника, синдрома раздраженного кишечника, ожирения и диабета 2 типа. Указанные соединения имеют общую формулу (1), где символы имеют значения, приведенные в описании. The present invention relates to arylsulfonylpyrazolinecarboxamidine derivatives as antagonists of 5-HT receptors, to methods for producing these compounds, and to new intermediates useful in their synthesis. In addition, the present invention relates to the use of these compounds and compositions, in particular their use for administration to patients in order to achieve a therapeutic effect in the treatment of Parkinson’s disease, Huntington’s chorea, schizophrenia, anxiety, depression, manic-depressive psychosis, psychoses, epilepsy, obsessive compulsive disorders, affective disorders, migraine, Alzheimer's disease, age-related cognitive impairment, ...

Arylsulfonyl pyrazoline carboxamidine derivatives as 5-HT6 antagonists

本发明涉及作为5-HT 6 受体的拮抗剂的芳基磺酰基吡唑啉甲脒衍生物，这些化合物的制备方法和可用于它们合成的新型中间体。本发明还涉及此类化合物和组合物的用途，尤其是它们施用于患者而在以下病症中获得治疗效果的用途：帕金森病、亨廷顿舞蹈病、精神分裂症、焦虑、抑郁症、躁狂抑郁症、精神病、癫痫症、强迫性障碍、心境障碍、偏头痛、阿尔茨海默氏病、年龄相关认知减退、轻度认知损害、睡眠障碍、饮食障碍、厌食症、贪食症、贪吃症、惊恐发作、静坐不能、注意力缺陷伴多动障碍、注意力缺陷障碍、由可卡因，酒精，烟碱或苯并二氮杂滥用引起的戒断症状、疼痛、与脊椎创伤或头部损伤有关的病症、脑积水、功能性肠紊乱、肠易激综合征、肥胖症和2型糖尿病。该化合物具有以下通式(1)：

Keratin fiber staining composition, keratin fiber dyeing process, multi-compartment device and use of a composition

New indazole derivatives process for their preparation and pharmaceutical compositions containing them.

Benzamides substituted for the treatment of arthropods

Compuestos de la fórmula (Ia")**Fórmula** donde D1 representa C-R11 o un heteroátomo seleccionado de N u O; D2 representa C-R11 o un heteroátomo seleccionado de N u O; D3 representa C o N; D4 representa C o N; D5 representa C-R11 o N; donde como máximo uno (1) o dos agrupamientos seleccionados de D1, D2, D3, D4 y D5 representan un heteroátomo; representa un sistema aromático; y R1 representa alquilo C1-C6 opcionalmente sustituido; los agrupamientos A1 representa C-H, A2 representa CR3 o N, A3 representa CR4, A4 representa C-H, B1 representa CR6 o N, B2 representa C-H, B4 representa C-H y B5 representa CR10 o N; R3, R4, R6 y R10 independientemente uno de otro representan H, halógeno, ciano, nitro, o alquilo C1-C6, cicloalquilo C3-C6, alcoxi C1-C6, N-alcoxi C1-C6-imino-alquilo C1-C3, alquil C1-C6-sulfanilo, alquil C1-C6-sulfinilo, alquil C1-C6-sulfonilo, N-alquil C1-C6-amino, N,N-di-alquil C1-C6-amino o N-alcoxi C1-C3-alquil C1-C4-amino o 1- pirrolidinilo en cada caso eventualmente sustituidos; si ninguno de los agrupamientos A2 y A3 representa N, R3 y R4 junto con el átomo de carbono al que están unidos, pueden formar un anillo de 5 o 6 miembros, que contiene 0, 1 o 2 átomos de N y/o 0 o 1 átomo de O y/o 0 o 1 átomo de S, o si ninguno de los agrupamientos A1 y A2 representa N, R2 y R3 junto con el átomo de carbono al que están unidos, pueden formar un anillo de 6 miembros, que contiene 0, 1 o 2 átomos de N; R8 representa alcoxi C1-C4 sustituido con flúor o alquilo C1-C4 sustituido con flúor; R11 independientemente uno de otro representa H, halógeno, ciano, nitro, amino o un alquilo C1-C6 , alquiloxi C1-C6, alquil C1-C6-carbonilo, alquil C1-C6-sulfanilo, alquil C1-C6-sulfinilo, alquil C1-C6-sulfonilo eventualmente sustituidos, preferentemente representa H; W representa O o S; Q representa H, formilo, hidroxi, amino o alquilo C1-C6, alquenilo C2-C6, alquinilo C2-C6, cicloalquilo C3-C6, heterocicloalquilo C1-C5, alcoxi C1-C4, alquil C1-C6-cicloalquilo C3-C6, ...

Treating diabetes with dipeptidyl peptidase-IV inhibitors

The present invention is directed to novel substituted dihydropyrrolopyrazoles of structural Formula I which are inhibitors of the dipeptidyl peptidase-N enzyme and which are useful in the treatment or prevention of diseases in which the dipeptidyl peptidase-IV enzyme is involved, such as diabetes and particularly Type 2 diabetes. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which the dipeptidyl peptidase IV enzyme is involved.

NEW PIRAZOL T * REVES, A PROCEDURE FOR THEIR PREPARATION AND THEIR USE AS HERBICIDES

1-Aryl-5-hydrazino-pyrazoles

Die Erfindung betrifft neue 1-Aryl-5-hydrazino-pyrazole der allgemeinen Formel (I), <IMAGE> in welcher R¹ für Wasserstoff oder Alkyl steht, R² für Cyano oder Nitro steht, R³ für Wasserstoff, für jeweils gegebenenfalls substituiertes Alkyl, Alkenyl, Alkinyl oder Cycloalkyl, für einen Rest -?-R<6> oder für einen Rest -SO2-R<7> steht, R<4> für Wasserstoff, für jeweils gegebenenfalls substituiertes Alkyl, Alkenyl, Alkinyl oder Cycloalkyl, für einen Rest -?-R<6> oder für einen Rest -SO2-R<7> steht, R<5> für Wasserstoff steht oder für den Fall, daß R<4> für Wasserstoff steht, auch für einen Rest -?-R<6>, für einen Rest -SO2-R<7>, oder für jeweils gegebenenfalls substituiertes Alkyl, Alkenyl, Alkinyl oder Cycloalkyl steht, wobei jeweils X für Sauerstoff oder Schwefel steht, R<6> für Wasserstoff, Alkyl, Alkoxy, Alkoxyalkyl, Alkylthio, Alkylthioalkyl, Alkylamino, Dialkylamino, Halogenalkyl, Alkenyl, Alkinyl, für gegebenenfalls substituiertes Cycloalkyl oder für jeweils gegebenenfalls substituiertes Aryl, Aryloxy, Arylthio oder Arylamino steht und R<7> für Alkyl, Hydroxyalkyl, Alkoxyalkyl, Halogenalkyl, Alkenyl, Alkinyl, Cycloalkyl oder für jeweils gegebenenfalls substituiertes Aralkyl oder Aryl steht und Ar für substituiertes Phenyl oder für gegebenenfalls substituiertes Pyridyl steht, mehrere Verfarhen zu ihrer Herstellung und ihre Verwendung als Herbizide. The invention relates to new 1-aryl-5-hydrazino-pyrazoles of the general formula (I), <IMAGE> in which R¹ is hydrogen or alkyl, R² is cyano or nitro, R³ is hydrogen, each optionally substituted alkyl, alkenyl , Alkynyl or cycloalkyl, represents a radical -? - R <6> or represents a radical -SO2-R <7>, R <4> represents hydrogen, for optionally substituted alkyl, alkenyl, alkynyl or cycloalkyl, for a radical -? - R <6> or represents a radical -SO2-R <7>, R <5> represents hydrogen or, if R <4> represents ...

Arylsulfonyl pyrazoline carboxamidine derivatives as 5-ht6 antagonists 5-ht6

PIPERIDINYLpyrazolOPYRIMIDINONES AND THE USE OF THEM

Se refiere a un compuesto de formula (I-A) o (I-B), donde: R1 es hidrogeno o alquilo C1-C5; R2 es hidrogeno, alquilo C1-C4, entre otros; R3 es hidrogeno, halogeno, entre otros. Tambien se refiere a un procedimiento para su preparacion. Dichos compuestos son piperidinilpirazolopirimidinonas sustituidas utiles en el tratamiento de sangrado agudo y recurrente en pacientes con o sin trastornos hemostaticos hereditarios o adquiridos Refers to a compound of formula (I-A) or (I-B), where: R1 is hydrogen or C1-C5 alkyl; R2 is hydrogen, C1-C4 alkyl, among others; R3 is hydrogen, halogen, among others. It also refers to a procedure for its preparation. Said compounds are substituted piperidinylpyrazolopyrimidinones useful in the treatment of acute and recurrent bleeding in patients with or without inherited or acquired hemostatic disorders.

Novel non-systemic tgr5 agonists

The present invention relates to sulfonamide compounds of formula (I) and formula (II), or a pharmaceutically acceptable salt thereof. The present sulfonamide compounds are useful non-systemic TGR5 agonists that can be used to treat diabetic diseases in human. The present invention provides a pharmaceutical composition containing sulfonamide compounds of formula (I) and formula (II) and a method of making as well as a method of using same in treating patients inflicted with metabolic disorders by administering same. The compounds of the present invention may be used in combination with additional anti-diabetic drugs.

INDAZOL DERIVATIVES

LA INVENCION SE REFIERE A COMPUESTOS DE FORMULA I Y A SUS SALES FARMACEUTICAMENTE ACEPTABLES, EN LA QUE R, R1 Y R2 SON COMO SE HAN DEFINIDO EN LA PRESENTE. LA INVENCION SE REFIERE ADEMAS A COMPOSICIONES FARMACEUTICAS QUE CONTIENEN, Y A PROCEDIMIENTOS DE UTILIZACION DE LOS COMPUESTOS DE FORMULA I, O DE SUS SALES ACEPTABLES, PARA LA INHIBICION DE LA FOSFODIESTERASA (PDE) TIPO IV O DE LA PRODUCCION DE FACTOR DE NECROSIS TUMORAL (TNF) EN UN MAMIFERO. LA INVENCION SE REFIERE ADEMAS A INTERMEDIOS QUE RESULTAN DE UTILIDAD EN LA PREPARACION DE COMPUESTOS DE FORMULA I. THE INVENTION REFERS TO COMPOUNDS OF FORMULA I AND ITS PHARMACEUTICALLY ACCEPTABLE SALTS, IN WHICH R, R1 AND R2 ARE AS DEFINED HEREIN. THE INVENTION FURTHER CONCERNS PHARMACEUTICAL COMPOSITIONS CONTAINING, AND PROCEDURES FOR THE USE OF THE COMPOUNDS OF FORMULA I, OR THEIR ACCEPTABLE SALTS, FOR THE INHIBITION OF TYPE IV PHOSFODIESTERASA (PDE) OR FACTOR PRODUCTION ) IN A MAMMAL. THE INVENTION FURTHER REFERS TO INTERMEDIATES RESULTING FROM USEFULNESS IN THE PREPARATION OF FORMULA I COMPOUNDS.

Pyrazolamide derivative serving as ep4 receptor antagonist and use thereof in preparation of drugs for treating cancer and inflammation

A compound capable of effectively antagonizing an EP4 receptor, which compound is a compound as represented by formula (I), and a tautomer, a stereoisomer, a hydrate, a solvate, a pharmaceutically acceptable salt or a prodrug thereof, wherein R 1 is selected from H or a halogen, and the halogen is selected from F, Cl, Br and I.

ARILSULFONIL PIRAZOLIN CARBOXAMIDINE DERIVATIVES AS 5-HT6 ANTAGONISTS

Esta invención se refiere a derivados de arilsulfonil pirazolin carboxamidina como antagonistas de receptores 5-HT6, a métodos para la preparación de estos compuestos y a novedosos intermediarios útiles para su síntesis. La invención también se refiere a los usos de tales compuestos y composiciones particularmente su uso en la administración de los mismos a pacientes para lograr un efecto terapéutico en la enfermedad de Parkinson, corea de Huntington, esquizofrenia, ansiedad, depresión, depresión maníaca, psicosis, epilepsia, trastornos obsesivos compulsivos, trastornos del ánimo, migraña, enfermedad de Alzheimer, declinación cognitiva relacionada con la edad, deterioro cognitivo leve, trastornos del sueño, trastornos de la alimentación, anorexia, bulimia, trastornos de atracones en la alimentación , ataques de pánico, acatisia, trastorno de hiperactividad y déficit de atención, trastorno de déficit de atención, abstinencia del abuso de cocaína, etanol, nicotina o benzodiazepinas, dolor, trastornos asociados con trauma espinal o daño en la cabeza, hidrocefalia, trastorno funcional del intestino, Síndrome de Intestino Irritable, obesidad y diabetes tipo 2. Los compuestos tienen la fórmula general (1): en donde los símbolos tienen los significados dados en la descripción.

Tlr7/tlr8抑制劑之晶型

本申請涉及處於其游離形式的( S) - N -(4-((5-(1,6-二甲基-1 H -吡唑并[3,4-b]吡啶-4-基)-3-甲基-4,5,6,7-四氫-1 H -吡唑并[4,3-c]吡啶-1-基)甲基)雙環[2.2.2]辛烷-1-基) 啉-3-甲醯胺的不同晶型，連同組成物、其製備方法、以及其使用方法。在一些實施方式中，晶型也含有水(“水合物”)。該等材料在不同自身免疫性疾病的治療中是有用的，該等自身免疫性疾病包括全身性紅斑狼瘡、皮膚狼瘡、盤狀狼瘡、混合性結締組織病、原發性膽汁性肝硬化、免疫性血小板減少性紫癜、化膿性汗腺炎、皮肌炎、多發性肌炎、乾燥綜合征、關節炎、類風濕關節炎和銀屑病。

피리다존 유도체의 제조방법

내용 없음.

Substituierte arylpyrazole als parasitizide

Ｔｌｒ７／ｔｌｒ８阻害剤の結晶形態

【課題】ＴＬＲ７及びＴＬＲ８の二重阻害剤である化合物の結晶形態、およびその結晶形態を含む医薬組成物、結晶形態を製造する方法並びにＴＬＲ７及びＴＬＲ８から選択されるエンドソームのトール様受容体の活性と関連する特定の自己免疫疾患を治療する方法を提供する。【解決手段】遊離形態である化合物（Ｓ）－Ｎ－（４－（（５－（１，６－ジメチル－１Ｈ－ピラゾロ［３，４－ｂ］ピリジン－４－イル）－３－メチル－４，５，６，７－テトラヒドロ－１Ｈ－ピラゾロ［４，３－ｃ］ピリジン－１－イル）メチル）ビシクロ［２．２．２］オクタン－１－イル）モルホリン－３－カルボキサミドの種々の結晶形態を提供する。いくつかの実施形態において、結晶形態は水も含む（水和物）。これらの材料は、全身性エリテマトーデス、皮膚ループス、円板状ループス、混合性結合組織病、原発性胆汁性肝硬変を含む種々の自己免疫疾患の治療に有用である。【選択図】なし

Ｔｌｒ７／ｔｌｒ８阻害剤の結晶形態

2H-indazolone compound

A novel 2H-indazolone-3 compound in the form of 3-( Beta morpholino-ethoxy)-4,5,6,7-tetrahydro-2H-indazole or the hydrobromide thereof. This compound is analgetically highly effective and may be produced in a high purity.

피리다존 및 피리다진 유도체의 제조방법

내용 없음

Synthesis of aromatic boronic acids

The invention relates to a method for the preparation of phenylboronic acids of formula (I), or combinations thereof, key intermediates in the preparation of compounds of interest in the agrochemical industry. The process comprises adding a borate over a Grignard reagent.

Indazole derivatives and pharmaceutical compositions containing them with the effect of inhibitors of phosphodiesterase (pde) type iv and the production of tumor necrosis factor (tnf)

Formas cristalinas de un inhibidor de tlr7/tlr8.

Esta solicitud se refiere a diversas formas cristalinas de (S)-N-(4-((5-(1,6-dimetil-1H-pirazolo[3,4-b]piridin-4-il)-3-metil -4,5,6,7-tetrahidro-1H-pirazolo[4,3-c]piridin-1-il)metil)biciclo[ 2.2.2]octan-1-il)morfolina-3-carboxamida en su forma libre, al igual que a composiciones, método de preparación y métodos de uso de dichas formas. En algunas formas de realización, las formas cristalinas además contienen agua ("hidratos"). Estos materiales son útiles en el tratamiento de diversas enfermedades autoinmunitarias, que incluyen lupus eritematoso sistémico, lupus cutáneo, lupus discoide, enfermedad mixta del tejido conectivo, cirrosis biliar primaria, púrpura trombocitopénica inmunitaria, hidradenitis supurativa, dermatomiositis, polimiositis, síndrome de Sjögren, artritis, artritis reumatoide y psoriasis.

Indazolszármazékok és azokat tartalmazó IV típusú foszfodiészteráz (PDE) inhibitor és tumor nekrózis faktor termelés gátló hatású gyógyszerkészítmények

A jelen találmány tárgyát azők az (I) általánős képletű vegyületek ésazők gyógyszerészetileg elfőgadható sói képezik, ahől a képletbenszereplő R, R1 és R2 jelentése az alábbi. A találmány tárgyát képezitővábbá emlősök esetében a IV típűsú főszfődiészterázők (PDEIV)inhibíciójára vagy a tűmőr nekrózis faktőr (TNF) termelés gátlásáraszőlgáló, (I) általánős képletű vegyületeket tartalmazógyógyszerkészítmények, valamint (I) általánős képletű vegyületeketfelhasználó eljárásők. A találmány tárgyát képezik az (I) általánősképletű vegyületek előállítására szőlgáló köztitermékek is. Az (I)általánős képletben R jelentése hidrőgénatőm, 1-9 szénatőmősalkilcsőpőrt, -(CH2)m(5-10 tagú heterőciklűs) csőpőrt, ahől mparaméter értéke 0-2, (1-6 szénatőmős alkőxi)-1-6 szénatőmszámúalkilcsőpőrt, 2-6 szénatőmszámú alkenilcsőpőrt vagy -(Z1)b(Z2)c(6-10)szénatőmszámú arilcsőpőrt, ahől b és c paraméter értéke egymástólfüggetlenül 0 vagy 1, Z1 jelentése 1-6 szénatőmszámú alkiléncsőpőrtvagy 2-6 szénatőmszámú alkeniléncsőpőrt, valamint Z2 jelentéseőxigénatőm, kénatőm, SO2 csőpőrt vagy NR12 csőpőrt, tővábbá ahől azemlített R csőpőrtők adőtt esetben 1-3 közötti számú szűbsztitűensselhelyettesítettek, amely szűbsztitűensek egymástól függetlenül a halő-,hidrőxi-, 1-5 szénatőmszámú alkil, 2-5 szénatőmszámú alkenil-, 1-6szénatőmszámú alkőxi-, triflűőrmetil-, nitrő-, -CO2R12, -C(O)NR12R13,-NR12R13 és -SO2NR12R13 csőpőrtők közül kerülnek kiválasztásra, R1jelentése hidrőgénatőm, 1-9 szénatőmszámú alkilcsőpőrt, 2-3szénatőmszámú alkenilcsőpőrt vagy fenilcsőpőrt, ahől az említettalkil, alkenil és fenil R1 csőpőrtők adőtt esetben 1-3 közötti számúszűbsztitűenssel helyettesítettek, amely szűbsztitűensek egymástólfüggetlenül a metil-, etil-, triflűőrmetil- és halőcsőpőrtők közülkerülnek kiválasztásra, R2 jelentése adőtt esetben helyettesítettalkőxi- vagy aminőcsőpőrt, -(C(O)NR12(CHR12)mC(O)NR12O(CH2)q(6-10szénatőmszámú arilcsőpőrt), -C(=NR32)NH(CH2)p(6-10 szénatőmszámúarilcsőpőrt, -C(O)NR8(CHR12)mC(O)NR12(CH2) ...

Mittel zum färben von keratinfasern enthaltend ein diamino-n,n-dihydropyrazolonderivat, einen kuppler und ein polyol

Process for preparing herbicide substituted pyrazole derivatives and herbicide compositions containing the same

Procedimiento para preparar composiciones herbicidas a base de pirazoles.

Process for preparing herbicide substituted pyrazole derivatives and herbicide compositions containing the same

Substituerte pyrazolforbindelser med herbicid virkning

[UNK]

Procedimiento para preparar composiciones herbicidas a base de pirazoles.

PROCEDIMIENTO PARA PREPARAR DERIVADOS DE PIRAZOL, DE FORMULA ESTRUCTURAL (I), EN LA QUE R ES HALOALQUILO C1 - C4; R ES ALQUILO C1 - C4, CICLOALQUILO C5 - C6, ARALQUILO C7 - C9, FENILO O NAFTILO; R ES ALQUILO C1 - C4, ALQUENILO C2 - C4 O ALQUILTIOALQUILO C2 - C6; R ES HIDROGENO, ALQUILO C1 - C4 O TRIHALOMETILO; E Y ES OXIGENO O AZUFRE.CONSISTE EN HACER REACCIONAR UN COMPUESTO DE FORMULA (II), EN LA QUE R, R, R E Y TIENEN LOS SIGNIFICADOS YA INDICADOS, CON UNA PARA-FORMALDEHIDO O CON UN COMPUESTO DE FORMULA RO. EL PRODUCTO DE LA REACCION OBTENIDO SE PUEDEOPCIONALMENTE HALOGENAR O ACILAR.DE APLICACION EN AGRICULTURA COMO HERBICIDAS.

제초제로 유용한 피라졸 화합물의 제조방법

내용 없음

Processo para a preparacao de 1-aril-5-hidrazino-pirazois,composicoes herbicidas,processos para combater ervas daninhas e para a preparacao de composicoes

1-아릴-5 하이드라지노- 피라졸의 제조방법

내용 없음

１−アリ−ル−５−ヒドラジノ−ピラゾ−ル類

(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。

Process for the preparation of pyrazole derivatives having an herbicidal effect

Process for the preparation of pyrazole derivatives having an herbicidal effect

Pyrazole derivatives,their preparation and their use as herbicides

Processo para a preparacao de derivados de pirazol composicoes herbicidas e processos para combater ervas daninhas e para preparar composicoes

Pyrazoles as human non-pancreatic secretary phospholipase A2 inhibitors

Pyrazoles as human non-pancreatic secretory phospholipase A2 inhibitors

Pyrazoles as human non-pancreatic secretory phospholipase A2 inhibitors

Pyrazoles as human non-pancreatic secretory phospholipase a2 inhibitors

Pirazoles como inhibidores de la fosfolipasa secretoria no pancreatica a2 humana

Un compuesto de la fórmula (I) en donde: R1 es fenil, isoquinolin-3-il, pirazinil, piridin-2-il, piridin-2-il sustituido en la posición 4 con -alquil (C1 -C4 ), alcoxil (C1 -C4 ), -CN ó -(CH2 )n CONH2 en donde n va de 0 - 2; R2 es fenil; fenil sustituido con 1 a 3 sustituyentes seleccionados del grupo conformado por -alquil (C1 -C4 ), -CN, halo, -NO2 , CO2 -alquil (C1 -C4 ), y CF3 ; naftil; tiofeno ó tiofeno sustituido con 1 a 3 grupos halo; R3| es hidrógeno; fenil; fenil-alquenil (C2 -C6 ); piridil; naftil; quinolinil; -alquil (C1 -C4 )- tiazolil; fenil sustituido con 1 ó 2 sustituyentes seleccionados del grupo conformado por -alquil (C1 -C4 ), -CN, -CONH2 , -NO2 , CF3 , halo, alcoxi (C1 -C4 ), CO2 -alquil (C1 -C4 ), fenoxi y SR4 en donde R4 es -alquil (C1 -C4 ) o halofenil; fenil sustituido con un sustituyente seleccionado del grupo conformado por -O(CH2 )p R5 en donde p va de 1 a 3 y R5 es -CN, -CO2 H, -CONH2 , o tetrazolil, fenil y -OR6 en donde R6 es ciclopentil, ciclohexenil ó fenilsustituido con halo o alcoxi (C1 -C4 );ó fenil sustituido con uno dos sustituyentes los cuales, tomados junto con el anillo fenílico al cual ligados, forman una anillo metilendioxi; ym va de 1 a 5;ó una sal farmacéuticamente aceptable de éste.

Pyrazole als humane nicht-pankreatische sekretorische phospholipase-a2-inhibitoren

인간 비-췌장 분비성 포스포리파제 ａ2 억제제로서의 피라졸

신규한 피라졸 중 일종은 패혈성 쇼크와 같은 상태를 치료하기 위해 지방산의 sPLA 2 매개된 방출을 억제하기 위한 상기 화합물의 용도와 함께 기재되어 있다.

Treating diabetes with dipeptidyl peptidase-iv inhibitors

The present invention is directed to novel substituted dihydropyrrolopyrazoles of structural Formula I which are inhibitors of the dipeptidyl peptidase-N enzyme and which are useful in the treatment or prevention of diseases in which the dipeptidyl peptidase-IV enzyme is involved, such as diabetes and particularly Type 2 diabetes. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which the dipeptidyl peptidase IV enzyme is involved.