АМИДИНОГИДРАЗОНПРОИЗВОДНЫЕ ИЛИ ИХ КИСЛОТНО-АДДИТИВНЫЕ СОЛИ И СРЕДСТВО, ОБЛАДАЮЩЕЕ ИНГИБИРУЮЩИМ ДЕЙСТВИЕМ НА ФЕРМЕНТ SAMDC

FIELD: medicine, since products has pharmaceutical activity. SUBSTANCE: new amidinohydrazone derivatives of formula 1 wherein radicals have corresponding meanings, and agent having inhibitory effect on enzyme SAMDC. Structure of the compound of formula 1: р 990с ПЧ Го РОССИЙСКОЕ АГЕНТСТВО ПО ПАТЕНТАМ И ТОВАРНЫМ ЗНАКАМ (19) ВИ” 2 066 311 ' 13) СЛ 57 МК С 07С 281/18, А 61 К 31/15 12) ОПИСАНИЕ ИЗОБРЕТЕНИЯ К ПАТЕНТУ РОССИЙСКОЙ ФЕДЕРАЦИИ (21), (22) Заявка: 92004359/04, 23.10.1992 (30) Приоритет: 07.05.1990 СН 1538/90 (46) Дата публикации: 10.09.1996 (56) Ссылки: Вюспет. ВарВу$. Кез Соттип. 46, 288, 1972. Восрвет. 218, р.945-947 (1984). (62) Первичная заявка, из которой выделена настоящая: 4895338/04 (71) Заявитель: Циба-Гейги АГ (СН) (72) Изобретатель: Ярослав Станек[СН], Ерг Фрей[СН], Ждорджо Караватти[СН] (73) Патентообладатель: Циба-Гейги АГ (СН) С1 (54) АМИДИНОГИДРАЗОНПРОИЗВОДНЫЕ ИЛИ ИХ КИСЛОТНО-АДДИТИВНЫЕ СОЛИ И СРЕДСТВО, ОБЛАДАЮЩЕЕ ИНГИБИРУЮЩИМ ДЕИСТВИЕМ НА ФЕРМЕНТ ЗАМОС (57) Реферат: Использование: в медицине, т.к. продукт обладает фармацевтической активностью. Сущность изобретения: новые амидиногидразонпроизводные Фф-лы 1, при соответствующих значениях радикалов и средство, обладающее ингибирующим действием на фермент ЗАМОС. Структура соединения ф-лы 1: х 1 2066311 табл. КО р 990с ПЧ Го КУЗЗАМ АСЕМСУ ГОК РАТЕМТ$ АМО ТКАОЕМАКК$ (19) (51) 1пЕ. С1.6 12) АВЗТКАСТ ОЕ 1МУЕМТОМ ВИ “” 2 066 311 ^^ Сл С 07 С 2811/16, А 61 К 31/15 (21), (22) АррИсаНоп: 92004359/04, 23.10.1992 (30) Рношу: 07.05.1990 СН 1538/90 (46) Рае ог рибИсаНоп: 10.09.1996 (62) Еа\ег аррйсаНоп: 4895338104 (71) АррИсапе: Тэфа-Сеа! Ас (СН) (72) пуетог. — Уагозау Запек[Г СН], Ега Егейсн], Пдога7По Кагауиа СН] (73) Ргорпеюг: Тэфа-Сеа! Ас (СН) (54) АМПОМОНУОКА?ОМЕ ОЕКМАТМЕ$ ОК АСШО АБОПОМ ЗАЕТ$ ТНЕВЕОР, АМО АСЕМТ НАММС МНЕТОКУ ЕРЕЕСТ ОМ ЕМХУМЕ ЗАМОС (57) АБзасЕ: НЕГО: тедсте, этсе ргодцб$ паз рпагтасеи!са! ас!уйу. ЗУВЗТАМСЕ: пем апатойпудгахопе 4епуаНуез ог Югтуца 1 \пегет гаЧ!са!$ пауе соггезропата теаппа$, ...

ТИОЭФИРНЫЕ СОЕДИНЕНИЯ В КАЧЕСТВЕ ИНГИБИТОРОВ НИТРИФИКАЦИИ

РОССИЙСКАЯ ФЕДЕРАЦИЯ (19) RU (11) (13) 2017 143 177 A (51) МПК C05G 3/08 (2006.01) ФЕДЕРАЛЬНАЯ СЛУЖБА ПО ИНТЕЛЛЕКТУАЛЬНОЙ СОБСТВЕННОСТИ (12) ЗАЯВКА НА ИЗОБРЕТЕНИЕ (21)(22) Заявка: 2017143177, 11.05.2016 (71) Заявитель(и): БАСФ СЕ (DE) Приоритет(ы): (30) Конвенционный приоритет: 12.05.2015 EP 15167357.1 (85) Дата начала рассмотрения заявки PCT на национальной фазе: 12.12.2017 (86) Заявка PCT: (87) Публикация заявки PCT: WO 2016/180859 (17.11.2016) R U (54) ТИОЭФИРНЫЕ СОЕДИНЕНИЯ В КАЧЕСТВЕ ИНГИБИТОРОВ НИТРИФИКАЦИИ (57) Формула изобретения 1. Применение тиоэфирного соединения формулы I A 2 0 1 7 1 4 3 1 7 7 A Адрес для переписки: 105082, Москва, Спартаковский пер., 2, стр. 1, секция 1, этаж 3, ЕВРОМАРКПАТ 2 0 1 7 1 4 3 1 7 7 EP 2016/060517 (11.05.2016) R U (43) Дата публикации заявки: 13.06.2019 Бюл. № 17 (72) Автор(ы): НАВЕ Барбара (DE), ДИКХАУТ Йоахим (DE), НЕСВАДБА Петер (CH), СИСАЙ Михирет Текесте (DE), ВИССЕМАЙЕР Александер (DE), ЦЕРУЛЛА Вольфрам (DE), ПАСДА Грегор (DE), ВОЛЛКВИСТ Олоф (CH), КУННИНГАМ Алан Франсис (CH) или его стереоизомера, соли, таутомера или N-оксида в качестве ингибитора нитрификации, в которой R1 и R2 независимо выбраны из Н и C1-С2-алкила; и в которой R3 представляет собой (i) C(=O)Ra, C(=O)ORa, C(=O)NRcRd, C(=N-OH)Ra, C(=N-OH)NRcRd, C(=N-Rb)Ra, C(= N-Rb)NRcRd, C(=N-Rx)Ra, или C(=N-Rx)NRcRd; или (ii) C1-C8-алкил, С3-С8-циклоалкил, С2-С8-алкенил, С3-С8-циклоалкенил, или С2-С8-алкинил, причем С-атомы этих групп в каждом случае могут быть незамещенными Стр.: 1 или могут нести 1, 2, 3, 4 или 5 одинаковых или разных заместителей, выбранных из галогена, CN, ORa, NO2, NRcRd, NRb(C=O)Ra, C(=O)Ra, C(=O)ORa, C(=O)NRcRd, S(O)nRa, и S(O)nNRcRd; или (iii) С6-С14-арил, С5-С14-гетарил, С6-С14-арил-С1-С2-алкил, или С5-С14-гетарил-С1 -С2-алкил, причем ароматические фрагменты в каждом случае могут быть незамещенными или могут нести 1, 2, 3, 4 или 5 одинаковых или разных заместителей, выбранных из галогена, CN, Rx, ORa, SRa, NRcRd, NRb(C=O)Ra, NRb(C=O)NRcRd, ...

Tricyclic compounds having activity specific for integrins, particularly avB3 integrins, method for preparing same, intermediates therefor, use of said compounds as drugs, and pharmaceutical compositions containing same.

The subject of the invention is the products of formula (I) : in which R-1, R2, R3 / £4,R5 and G are as defined in the description, the dotted lines represent an optional second bond, as well as the addition salts with acids and bases and the esters, their preparation process and the intermediates of this process, their use as medicines and the pharmaceutical compositions containing them.

Tric clic ompou ds ha ing a tivity specific for integrins particularly avbs intergrins method for preparing same intermediates therefore use of said compounds as drugs and pharmaceutical compositions containing same

Anti-parasitic compounds and methods of their use

Tricyclic compounds having an activity screw-with-visdes intégrines in particular with respect to the intégrine ALPHAvBETA3, their method of preparation and I ntermédiaires of this process, their application as drugs and the compositions pharmaceutical containing them.

Tric clic ompou ds ha ing a tivity specific for integrins particularly avbs intergrins method for preparing same intermediates therefore use of said compounds as drugs and pharmaceutical compositions containing same

Anti-parasitic compounds and methods of their use

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

Thioether compounds as nitrification inhibitors

Abstract The invention concerns the use of thioether compounds of formula I as nitrification inhibitors, and agricultural mixtures and compositions comprising said thioether compounds. 16683457_1 (GHMatters) P43492.AU.1 ...

HETEROCYCLIC GUANIDINES

Elevation of hdl cholesterol by 2-(4-chloro -1-aryl-butylidene) -hydrazinecarbothioamides

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

Process for the preparation of asymmetrical bis(thiosemicarbazones)

The present invention relates to a method of making asymmetrical bis(thiosemicarbazones), compounds useful as synthetic intermediates in the method, new bis(thiosemicarbazones) that can be readily accessed by use of the method and methods of treatment and imaging utilising some of the new bis(thiosemicarbazones).

Hydrazone derivatives

Tricyclic compounds having activity specific for integrins, particularly alphav beta3 integrins, method for preparing same, intermediates therefor, use of said compounds as drugs, and pharmaceutical compositions containing same

COMPOUNDS AND METHODS OF TREATING INFECTIONS

The invention provides compounds of Formula (l), and methods of treating or preventing a bacterial infection in a subject using a compound of Formula (l). The invention also provides the use of a compound of Formula (l) in the manufacture of a medicament for the treatment of a bacterial infection in a subject. The invention further provides a medical device when used in a method of treating or preventing a bacterial infection in a subject and to a medical device comprising the composition of the invention.

COMPOSITIONS AND METHODS FOR NON-INVASIVE IMAGING

The present invention relates to a novel composition useful in targeted diagnostic and/or therapy of a target site, such as cancerous tissue. The composition and methods disclosed herein find particular use in diagnosing and imaging cancerous tissue. The present invention provides a new diagnostic tool for the utilization of positron emission tomography (PET) imaging technique.

COMPOUNDS AND METHODS OF TREATING INFECTIONS

The invention provides compounds of Formula (I), and methods of treating or preventing a bacterial infection in a subject using a compound of Formula (I). The invention also provides the use of a compound of Formula (I) in the manufacture of a medicament for the treatment of a bacterial infection in a subject. The invention further provides a medical device when used in a method of treating or preventing a bacterial infection in a subject and to a medical device comprising the composition of the invention.

SMALL MOLECULES FOR THE MODULATION OF MCL-1 AND METHODS OF MODULATING CELL DEATH, CELL DIVISION, CELL DIFFERENTIATION AND METHODS OF TREATING DISORDERS

This invention relates to compounds which selectively bind to the survival protein MCL-1 with high affinity and selectivity, pharmaceutical compositions containing such compounds and the use of those compounds or compositions for modulating MCL-1 activity and for treating hyperproliferative disorders, angiogenesis disorders, cell cycle regulation disorders, autophagy regulation disorders, inflammatory disorders, and/or infectious disorders and/or for enhancing cellular engraftment and/or wound repair, as a sole agent or in combination with other active ingredients.

MULTICATALYTIC PROTEASE INHIBITORS

Disclosed herein are inhibitors of the multicatalytic protease enzyme which are represented by general formula (I). Constituent members and preferred constituent members are disclosed herein. Methodologies for making and using the disclosed compounds are also set forth herein.

Verfahren zur Herstellung des Diäthanolaminsalzes der Benzaldehydthiosemicarbazon-4-carbonsäure.

Verwendung von Thiosemicarbazonen von ungesättigten Aldehyden zum antimikrobiellen Ausrüsten von Textilien bzw. zum Schützen von Textilien gegen Mikroorganismen

БИЦИКЛИЧЕСКИЕ АМИНОПРОИЗВОДНЫЕ И СОДЕРЖАЩИЕ ИХ АНТАГОНИСТЫ PGD2

АНТИБАКТЕРИАЛЬНЫЕ АГЕНТЫ

Предложены антибактериальные соединения формулы (I) а также их стереоизомеры или фармацевтически приемлемые соли; фармацевтические композиции, включающие такие соединения; способы лечения бактериальных инфекций введением таких соединений.

ТРИЦИКЛИЧЕСКИЕ СОЕДИНЕНИЯ, ОБЛАДАЮЩИЕ АКТИВНОСТЬЮ В ОТНОШЕНИИ ИНТЕГРИНОВ, В ЧАСТНОСТИ В ОТНОШЕНИИ ИНТЕГРИНА АЛЬФАvБЕТА 3, СПОСОБ ИХ ПОЛУЧЕНИЯ И ПРОМЕЖУТОЧНЫЕ СОЕДИНЕНИЯ, ИСПОЛЬЗУЕМЫЕ В ЭТОМ СПОСОБЕ, ИХ ПРИМЕНЕНИЕ В КАЧЕСТВЕ МЕДИКАМЕНТОВ И СОДЕРЖАЩИЕ ИХ ФАРМАЦЕВТИЧЕСКИЕ КОМПОЗИЦИИ

... 1. Соединения общей формулы (I) в которой R1обозначает группу -О-[А]-[В]-COR6, в которой R6обозначает -ОН, C1-С6алкокси, -О-СН2-СН(ОН)-СН2OН, [A] обозначает группу C1-С6алкилен, возможно замещенный оксогруппой, [B] обозначает радикал -CH(Z)- или простую связь, Z обозначает группу -NHCO2Rc, или -NHSO2Rc, где Rcобозначает радикал фенил(C1-С4)алкил-, хинолинил или пиридинилимидазолил(C1-С4)алкил-, R2и R3, одинаковые или разные, обозначают атом водорода, радикал гидроксил, радикал C1-С6алкокси или R2и R3образуют вместе группу -O-(C1-С3-алкилен)-O- или -O-C(Ph)2-O, G обозначает радикал -NH-C-(=X)-NH2, в котором Х обозначает S, О или NH, или радикал -NH-Het', где Het' обозначает имидазол, возможно замещенный группой оксо, пиримидин, диазепин или бензимидазол формул где р равно 2, 3 или 4, пунктирные линии представляют собой возможную вторую связь, а также соли присоединения с кислотами и основаниями и сложные эфиры, R1, R2и R3могут находиться в положении 8, 9 или 10 трицикла. 2. Соединения общей ...

Tricyclic Compounds Having Activity Specific for Integring, Particularly , avB3 Integrins, Method for Preparation the Same as Drugs and Pharmaceutical Composition Containing Same

Iron Chelators as HIV-1 Inhibitors

The present invention relates to chelator compounds for chelating metal ions. In particular, the present invention relates to (thio)semicarbazone compounds and (thio)hydrazone compounds, such as PpYeT and PpYaT, which are chelators for metal ions, including iron ions. Therapeutic use of such compounds and/or their metal ion complexes, includes methods for treating and inhibiting HIV-1 replication, particularly in HIV-1 infected cells.

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

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

Thio semicarbazone and semicarbozone inhibitors of cysteine proteases and methods of their use

The present invention relates to thio semicarbazone and semicarbazone inhibitors of cysteine proteases and methods of using such compounds to prevent and treat protozoan infections such as trypanosomiasis, malaria and leishmaniasis. The compounds also find use in inhibiting cysteine proteases associated with carcinogenesis, including cathepsins B and L.

HYDRAZONE.

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

MEANS FOR THE FIGHT AGAINST EKTOPARASITI HARMING INSECTS AND YOUR USE

TRIZYCLI CONNECTIONS WITH EFFECT ON INTEGRINE, PARTICULARLY ON THE ALPHAVBETA3-INTEGRIN, PROCEDURE FOR YOUR PRODUCTION AND INTERMEDIATE PRODUCTS OF THE PROCEDURE, YOUR USE AS DRUGS AND IT ABSTENTION PHARMACEUTICAL COMPOSITIONS

Elevation of hdl cholesterol by 4-{(aminothioxomethyl) -hydrazono} -n-(substituted) -4-arylbutanamides

Dithiocarbazonic acid derivatives as pesticides

Compounds for treatment of proliferative disorders

Small molecules for the modulation of MCL-1 and methods of modulatiing cell death, cell division, cell differentiation and methods of treating disorders

This invention relates to compounds which selectively bind to the survival protein MCL-1 with high affinity and selectivity, pharmaceutical compositions containing such compounds and the use of those compounds or compositions for modulating MCL-1 activity and for treating hyperproliferative disorders, angiogenesis disorders, cell cycle regulation disorders, autophagy regulation disorders, inflammatory disorders, and/or infectious disorders and/or for enhancing cellular engraftment and/or wound repair, as a sole agent or in combination with other active ingredients.

ANTIBACTERIAL AGENTS

... ²²²Antibacterial compounds of formula (I) are provided: As well as stereoisomers, ²pharmaceutically acceptable salts, esters, and prodrugs thereof; ²pharmaceutical compositions comprising such compounds; methods of treating ²bacterial infections by the administration of such compounds; and processes ²for the preparation of the compounds.² ...

COMPOSITIONS AND METHODS FOR ENHANCING VIRUS EFFICACY

Provided are viral sensitizing compounds that enhance the efficacy of viruses by increasing spread of the virus in cells, increasing the titer of virus in cells, or increasing the cytotoxicity of virus to cells. Other uses, compositions and methods of using same are also provided.

ANTIBACTERIAL AGENTS

PROCESSES AND COMPOSITIONS FOR the BREEDING OF the ANIMALS

NEW COMPOSE TRICYCLIC, THEIR METHOD OF PREPARATION, AND THEM INTERMEDIARIES OF THIS PROCESS, THEIR APPLICATION AS DRUGS AND THE COMPOSITIONS PHARMACEUTICAL CONTAINING THEM

Compounds of formula (I), wherein R1, R2, R3, R4, R5 and G are as defined in the description and the dotted lines indicate an optional second bond, as well as the acid, base and ester addition salts thereof, a method for preparing said compounds, intermediates therefor, the use of said compounds as drugs, and pharmaceutical compositions containing same, are disclosed.

Composto composições e métodos

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

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

ANTI-PARASITIC COMPOUNDS AND METHODS OF THEIR USE

The present invention provides a novel class of compounds that disrupt the parasitic infectious life cycle and serve as promising agents for anti-parasitic therapy.

Antibacterial agents

Antibacterial compounds of formula I are provided: As well as stereoisomers, pharmaceutically acceptable salts, esters, and prodrugs thereof; pharmaceutical compositions comprising such compounds; methods of treating bacterial infections by the administration of such compounds; and processes for the preparation of the compounds.

Metal Complexes and Methods of Treatment

In one embodiment, the present application discloses compounds that are selective neuroactive agents for the treatment of diseases of the central nervous system (CNS). In one aspect, the neuroactive agents are NCDs of metal chelates, including complexes of iron, copper or zinc. 2. The NCD of wherein:{'sup': 3', '4', '1', '2, 'sub': 1', '6', '5', '10', '1', '6', '6-10', '1', '6', '1', '6', '1-2', '1', '6', '1', '6, 'Rand Rare each independently H, substituted or unsubstituted C-Calkyl, substituted or unsubstituted C-Caryl, substituted or unsubstituted —C-Calkyl-Caryl, substituted or unsubstituted C-CalkylC(O)—, substituted or unsubstituted C-CalkylS(O)—, substituted or unsubstituted C-CalkylNR′C(O)— and substituted or unsubstituted C-CalkoxyC(NR″)—, or Rand Rtogether with the carbon atoms that they are attached to form a 5 or 6-membered carbocyclic ring;'}{'sup': 1', '2, 'sub': 1', '6', '5', '10', '1', '6', '6', '10', '1', '6', '1', '6', '1', '6', '1-2', '1', '6', '1', '6, 'Ris H and Ris selected from the group consisting of substituted or unsubstituted C-Calkyl, substituted or unsubstituted C-Caryl, substituted or unsubstituted —C-Calkyl-C-Caryl, substituted or unsubstituted heterocyclyl, —C-Calkyl-heterocyclyl, substituted or unsubstituted C-CalkylC(O)—, substituted or unsubstituted C-CalkylS(O)—, substituted or unsubstituted C-CalkylNR′C(O)— and substituted or unsubstituted C-CalkoxyC(NR″)—; and'}{'sup': 5', '6, 'sub': 1', '6', '5', '10', '1', '6', '6', '10', '1', '6', '1', '6', '1', '6', '1-2', '1', '6', '1', '6, 'Ris H and Ris selected from the group consisting of substituted or unsubstituted C-Calkyl, substituted or unsubstituted C-Caryl, substituted or unsubstituted —C-Calkyl-C-Caryl, substituted or unsubstituted heterocyclyl, —C-Calkyl-heterocyclyl, substituted or unsubstituted C-CalkylC(O)—, substituted or unsubstituted C-CalkylS(O)—, substituted or unsubstituted C-CalkylNR′C(O)— and substituted or unsubstituted C-CalkoxyC(NR″)—.'}3. The NCD of claim 1 , ...

СОЕДИНЕНИЯ И СПОСОБЫ ЛЕЧЕНИЯ ИНФЕКЦИЙ

FIELD: chemistry. SUBSTANCE: invention relates to particular compounds enumerated in claim 1. Invention also relates to an antibacterial pharmaceutical composition containing said compounds and their use in the manufacture of a medicament for treating or preventing bacterial colonization or infection in a subject, said bacterial infection being caused by a bacterial agent. EFFECT: compounds may find use for treatment or prevention of bacterial colonization or infection in a subject. 19 cl, 41 dwg, 47 tbl, 12 ex РОССИЙСКАЯ ФЕДЕРАЦИЯ (19) RU (51) МПК C07C 281/08 C07C 281/18 C07C 323/45 C07C 337/08 C07D 209/14 C07D 209/40 ФЕДЕРАЛЬНАЯ СЛУЖБА C07D 213/53 ПО ИНТЕЛЛЕКТУАЛЬНОЙ СОБСТВЕННОСТИ C07D 215/12 C07D 239/50 C07D 249/14 (12) (11) (2006.01) (2006.01) (2006.01) (2006.01) (2006.01) (2006.01) (2006.01) (2006.01) (2006.01) (2006.01) (13) 2 666 540 C2 C07D 251/66 (2006.01) C07D 295/125 (2006.01) C07D 307/56 (2006.01) C07D 333/58 (2006.01) A01N 43/54 (2006.01) A01N 47/44 (2006.01) A61K 31/14 (2006.01) A61K 31/155 (2006.01) A61K 31/17 (2006.01) A61K 31/175 (2006.01) ОПИСАНИЕ ИЗОБРЕТЕНИЯ К ПАТЕНТУ (52) СПК 2015150264, 01.05.2014 (24) Дата начала отсчета срока действия патента: 01.05.2014 Дата регистрации: 11.09.2018 (73) Патентообладатель(и): НЕОКУЛИ ПТИ ЛТД (AU) Приоритет(ы): (30) Конвенционный приоритет: (43) Дата публикации заявки: 05.06.2017 Бюл. № 3992446 A, 16.11.1976. US 4754067 A, 28.06.1988. US 3941825 A, 02.03.1976. US 4575560 A, 11.03.1986. WO 2005/031000 A2, 07.04.2005. CAS RN 1024798-17-1 (дата ввода 03.06.2008) (получено из STN). CAS RN 902275-25-6 (дата ввода 17.08.2006) (получено из STN). CAS RN 387363-92-0 (дата ввода 28.01.2002) (получено из STN). (см. прод.) 16 (45) Опубликовано: 11.09.2018 Бюл. № 26 2 6 6 6 5 4 0 (56) Список документов, цитированных в отчете о поиске: GB 1304164 A, 24.01.1973. US (85) Дата начала рассмотрения заявки PCT на национальной фазе: 01.12.2015 (86) Заявка PCT: AU 2014/000483 (01.05.2014) (87) Публикация заявки PCT: WO 2014/176636 ( ...

СПОСОБЫ ЛЕЧЕНИЯ ПРОТОЗОЙНЫХ ИНФЕКЦИЙ

FIELD: medicine.SUBSTANCE: group of inventions refers to treatment or prevention of protozoal infection in a subject. That is ensured by using a compound or its pharmaceutically acceptable salt selected from: NCL015, NCL016, NCL017, NCL020, NCL021, NCL022, NCL023, NCL024, NCL025, NCL026, NCL027, NCL028, NCL029, NCL030, NCL031, NCL032, NCL033, NCL034, NCL035, NCL036, NCL037, NCL038, NCL039, NCL040, NCL041, NCL042, NCL043, NCL044, NCL045, NCL046, NCL052, NCL053, NCL054, NCL062, NCL072, NCL073, NCL074, NCL075, NCL076, NCL077, NCL078, NCL079, NCL080, NCL081, NCL082, NCL083, NCL084, NCL085, NCL086, NCL087, NCL088, NCL089, NCL093, NCL094, NCL096, NCL097, NCL099, NCL100, NCL101, NCL102, NCL103, NCL107, NCL108, NCL109, NCL110, NCL112, NCL113, NCL114, NCL115, NCL116, NCL117, NCL118, NCL119, NCL120, NCL121, NCL123, NCL125, NCL126, NCL127, NCL129, NCL130, NCL131, NCL132, NCL133, NCL134, NCL135, NCL136, NCL137, NCL138, NCL139, NCL140, NCL141, NCL143, NCL144, NCL145, NCL146, NCL147, NCL150, NCL151, NCL152, NCL153, NCL154, NCL155, NCL156, NCL160, NCL164, NCL165, NCL166, NCL170, NCL171, NCL172, NCL174, NCL175, NCL176, NCL177, NCL188, NCL190, NCL191, NCL215, NCL216, NCL217, NCL219, NCL224, NCL225, NCL226, NCL228, NCL229, NCL231, NCL232, NCL233, NCL234, NCL235, NCL236, NCL237, NCL248, NCL249, NCL254, NCL257, NCL259, NCL261, NCL263, NCL265, NCL266, NCL271, NCL272, NCL273, NCL274. Group of inventions relates to use of a compound or a pharmaceutically acceptable salt, to an antiprotozoal pharmaceutical composition containing a compound, as well as to a medical device containing the composition.EFFECT: invention provides extending the range of products for treating or preventing protozoal infection in a subject.19 cl, 13 dwg, 9 tbl, 14 ex РОССИЙСКАЯ ФЕДЕРАЦИЯ (19) RU (11) (51) МПК A61K 31/155 (2006.01) A61K 31/17 (2006.01) A61K 31/4045 (2006.01) A61K 31/4192 (2006.01) A61K 31/341 (2006.01) A61K 31/498 (2006.01) ФЕДЕРАЛЬНАЯ СЛУЖБА A61K 31/44 (2006.01) ПО ИНТЕЛЛЕКТУАЛЬНОЙ СОБСТВЕННОСТИ ...

Способ получения тиосемикарбазон-силикагеля

Изобретение относится к получению сорбционных материалов на основе ковалентно модифицированных силикагелей. Предложен способ получения силикагеля, ковалентно модифицированного тиосемикарбазонными группами, путём взаимодействия силикагеля, содержащего ковалентно иммобилизованный фрагмент с альдегидной группой, и тиосемикарбазида в среде этанола при нагревании при 80°С в течение 1 ч в присутствии каталитического количества соляной кислоты. Технический результат – расширение ассортимента сорбционных материалов на основе силикагелей. 1 пр.

NOVEL BICYCLO(2,2,1)HEPTYL-5-HEPTENOIC ACID THROMBOXANE A2 ANTAGONISTS

This invention relates to novel optically active thromboxane A2 inhibiting 7-?3- ?1-??(phenylamino)thioxomethyl!hydrazono!ethyl!-bicyclo?2,2,1! heptenoic acids and to methods for their manufacture.

BIZYKLI AMINODERIVATE AND CONTAINING PGD2 ANTAGONIST

MULTI-CATALYTIC PROTEASE INHIBITORS

KATECHOLHYDRAZON DERIVATIVES, PROCEDURES FOR YOUR PRODUCTION AND PHARMACEUTICAL COMPOSITIONS THIS CONTAINING

TECHNETIUM-99M-KOMPLEXE FOR USE AS RADIO-PHARMACEUTICAL MEANS

Elevation of hdl cholesterol by n-{2-{ (aminothioxomethyl)hydrazono} -2-arylethyl}amides

BENT AND COSMETICS CONTAINING SAID POLYSTYRENE DERIVATIVE AS ACTIVE INGREDIENT

Ectoparasitic insect pest controllers for animals and their usage

TICALS

Metal complexes and methods of treatment

In one embodiment, the present application discloses compounds that are selective neuroactive agents for the treatment of diseases of the central nervous system (CNS). In one aspect, the neuroactive agents are NCDs of metal chelates, including complexes of iron, copper or zinc.

ARYLHYDRAZONES

QUINONE DERIVATIVES FOR USE IN ANIMAL HUSBANDRY

Bisubstituted carbocyclic cyclophilin binding compounds and theirus

CATHECOL HYDRAZONE DERIVATIVES, PROCESS FOR PREPARING THE SAME AND PHARMACEUTICAL COMPOSITION CONTAINING THE SAME

The present invention provides novel cathecol hydrazone derivatives of formula (I) or pharmaceutically acceptable salts thereof, wherein R1 is C1-7 alkyl or C3-7 cycloalkyl; R2 is hydrogen, hydroxy, C1-5 alkyl or -CH2CH2C(=O)NH2; R3 and R4 are independently hydrogen, C1-7 alkyl, -C(=X)-R5, or 2-, 3- or 4- pyridyl, prymidyl or phenyl substituted with one or two selected from a group consisting of halogen, C1-6 alkoxy, nitro, trifluoromethyl, C1-6 alkyl and carboxyl, or R3 and R4 are directly bonded by C3-4 containing oxygen, sulfur or nitrogen to form a heterocyclic ring, X is oxygen, sulfur or NH and R5 is C1-7 alkyl, -NHR6, CONH2 or 2-, 3- or 4-pyridyl, prymidyl or phenyl substituted with one selected from a group consisting of halogen, C1-6 alkoxy, nitrile, trifluoromethyl, C1-6 alkyl and carboxyl, and R6 is hydrogen, hydroxy, NH2, C1-5 alkoxy, C1-5 alkyl, pyridyl or phenyl.

ANTINEOPLASTIC COMPOUNDS AND PHARMACEUTICAL COMPOSITIONS THEREOF

The invention relates to chemical compounds which are obtained by means of in silico molecular modelling and which have a structure that can be used to block phosphorylation by interacting said compounds with the phosphorylation domain or the environment thereof in the substrates of the Casein Kinase II enzyme. The invention also relates to pharmaceutical compositions that contain said compounds and to the use thereof in the preparation of medicaments for the treatment of diseases associated with neoplastic processes.

METHODS FOR TREATING PROTOZOAN INFECTIONS

The invention provides compounds of Formula (I), and their use in methods for treating or preventing a protozoan infection in a subject using a compound of Formula (I). The invention also provides the use of a compound of Formula (I) in the manufacture of a medicament for the treatment of a protozoan infection in a subject. The invention further provides a medical device when used in a method of treating or preventing a protozoan infection in a subject and to a medical device comprising the composition of the invention.

COMPOSITIONS AND METHODS FOR INHIBITION OF CATHEPSINS

This invention is directed to compound of Formula I and methods of using these compounds in the treatment of conditions in which modulation of a cathepsin, particularly cathepsin K or cathepsin L, will be therapeutically useful.

CATHECOL HYDRAZONE DERIVATIVES, PROCESS FOR PREPARING THE SAME AND PHARMACEUTICAL COMPOSITION CONTAINING THE SAME

The present invention provides novel cathecol hydrazone derivatives of formu la (I) or pharmaceutically acceptable salts thereof, wherein R1 is C1-7 alkyl o r C3-7 cycloalkyl; R2 is hydrogen, hydroxy, C1-5 alkyl or -CH2CH2C(=O)NH2; R3 and R4 are independently hydrogen, C1-7 alkyl, -C(=X)-R5, or 2-, 3- or 4- pyridyl, prymidyl or phenyl substituted with one or two selected from a grou p consisting of halogen, C1-6 alkoxy, nitro, trifluoromethyl, C1-6 alkyl and carboxyl, or R3 and R4 are directly bonded by C3-4 containing oxygen, sulfur or nitrogen to form a heterocyclic ring, X is oxygen, sulfur or NH and R5 is C1-7 alkyl, -NHR6, CONH2 or 2-, 3- or 4-pyridyl, prymidyl or phenyl substituted with one selected from a group consisting of halogen, C1-6 alkox y, nitrile, trifluoromethyl, C1-6 alkyl and carboxyl, and R6 is hydrogen, hydroxy, NH2, C1-5 alkoxy, C1-5 alkyl, pyridyl or phenyl.

COMPOUNDS FOR TREATMENT OF PROLIFERATIVE DISORDERS

Disclosed are compounds of formula (IA), formula (IV) or formula (V), whe rein the variables are as defined herein, and pharmaceutical compositions co ntaining them which are useful for treating a subject with a proliferative d isorder, such as cancer. The disclosed compounds and pharmaceutical composit ions are also useful for treating disorders responsive to Hsp70 induction an d/or natural killer induction.

PROCESS FOR THE PREPARATION OF ASYMMETRICAL BIS(THIOSEMICARBAZONES)

The present invention relates to a method of making asymmetrical bis(thiosemicarbazones), compounds useful as synthetic intermediates in the method, new bis(thiosemicarbazones) that can be readily accessed by use of the method and methods of treatment and imaging utilising some of the new bis(thiosemicarbazones).

HETEROCYCLIC SUBSTITUTED GUANIDINES

HETEROCYCLIC SUBSTITUTED GUANIDINES

TRICYCLIC COMPOUNDS HAVING ACTIVITY SPECIFIC FOR INTEGRINS, PARTICULARLY 'alpha'v'beta'3 INTEGRINS, METHOD FOR PREPARING SAME, INTERMEDIATES THEREFOR, USE OF SAID COMPOUNDS AS DRUGS, AND PHARMACEUTICAL COMPOSITIONS CONTAINING SAME

Compounds of formula (I), wherein R1, R2, R3, R4, R5 and G are as defined in the description and the dotted lines indicate an optional second bond, as well as the acid, base and ester addition salts thereof, a method for preparing said compounds, intermediates therefor, the use of said compounds as drugs, and pharmaceutical compositions containing same, are disclosed.

COMPOUNDS AND METHODS OF TREATING INFECTIONS

The invention provides compounds of Formula (I), and methods of treating or preventing a bacterial infection in a subject using a compound of Formula (I). The invention also provides the use of a compound of Formula (I) in the manufacture of a medicament for the treatment of a bacterial infection in a subject. The invention further provides a medical device when used in a method of treating or preventing a bacterial infection in a subject and to a medical device comprising the composition of the invention.

Novel methods of manufacturing thromboxane A2 antagonists

Hydrazones

TECHNETIUM-99M-KOMPLEXE ZUR VERWENDUNG ALS RADIOPHARMAZEUTISCHE MITTEL

Mittel zur Bek{mpfung von Ektoparasitischen Schadeinsekten und ihre Verwendung

ARYLHYDRAZONE.

HYDRAZONDERIVATE AS PESTICIDES

Hydrazones

Compositions and methods for non-invasive imaging

The present invention relates to a novel composition useful in targeted diagnostic and/or therapy of a target site, such as cancerous tissue. The composition and methods disclosed herein find particular use in diagnosing and imaging cancerous tissue. The present invention provides a new diagnostic tool for the utilization of positron emission tomography (PET) imaging technique.

ANTINEOPLASTIC COMPOUNDS AND PHARMACEUTICAL COMPOSITIONS THEREOF

... ²²²The invention relates to chemical compounds which are obtained by means of in ²silico molecular modelling and which have a structure that can be used to ²block phosphorylation by interacting said compounds with the phosphorylation ²domain or the environment thereof in the substrates of the Casein Kinase II ²enzyme. The invention also relates to pharmaceutical compositions that contain ²said compounds and to the use thereof in the preparation of medicaments for ²the treatment of diseases associated with neoplastic processes.² ...

ARYLHYDRAZONES

Compounds of formula I (see formula I) wherein A, X1, X2, X3, X4, Y, Z and R1 to R6 have the meanings given in the description, have valuable pharmaceutical properties and are effective especially against tumours. They are prepared in a manner known per se.

BISUBSTITUTED CARBOCYCLIC CYCLOPHILIN BINDING COMPOUNDS AND THEIR USE

The present invention relates to novel, non-peptidic small organic compounds having an affinity for cyclophilin (CyP)-type immunophilin proteins. In the compounds of this invention, at least two carbo-or heterocyclic groups are attached to a central saturated, partially saturated, or aromatic 5-6 membered carbocyclic ring by a combination of straight or branched linker chains. The invention further relates to pharmaceutical compositions comprising one or more of the said compounds, and to the uses of these compounds and compositions for binding CyP-type proteins, inhibiting their peptidyl-prolyl isomerase activity, and for research, development, and therapeutic applications in a variety of medical disorders, such as neurological disorders, hair loss disorders, ischemic disorders, and disorders caused by viral or protozoan infection.

ANTIBACTERIAL AGENTS

Antibacterial compounds of formula (I) are provided: As well as stereoisomers, pharmaceutically acceptable salts, esters, and prodrugs thereof; pharmaceutical compositions comprising such compounds; methods of treating bacterial infections by the administration of such compounds; and processes for the preparation of the compounds.

HYDRAZONE DERIVATIVES

Compounds of formula (I), wherein m, n, R1, R2, R3, R4, R17 and X are as defined in claim 1, and, as the case may be, tautomers thereof, in each case in free form or in salt form, can be used as agrochemical active ingredients and can be prepared in a manner known per se.

PROCESS FOR THE PREPARATION OF ASYMMETRICAL BIS(THIOSEMICARBAZONES)

Compositions and methods for enhancing viral efficacy

METHODS FOR TREATING PROTOZOAN INFECTIONS

PROTECTIVE MOLECULES AGAINST ANTHRAX TOXIN

Disclosed herein inter alia are compositions and methods useful in the treatment of infectious diseases and exposure to toxins.

Hydrazones

Compounds of formula I (I) wherein A, X, Z and R1-R5 are as defined in the description, and their salts have valuable pharmaceutical properties and are effective especially against tumors. They are prepared in a manner known per se.

Antibacterial agents

Antibacterial compounds of formula I are provided: As well as stereoisomers, pharmaceutically acceptable salts, esters, and prodrugs thereof; pharmaceutical compositions comprising such compounds; methods of treating bacterial infections by the administration of such compounds; and processes for the preparation of the compounds.

COMPOSITIONS AND METHODS FOR ENHANCING VIRUS EFFICACY

Provided are viral sensitizing compounds that enhance the efficacy of viruses by increasing spread of the virus in cells, increasing the titer of virus in cells, or increasing the cytotoxicity of virus to cells. Other uses, compositions and methods of using same are also provided.

Hydrazones

Compounds of the formula I in which A denotes a direct bond or -(CH2)n-, in which n represents 1, 2 or 3; X represents a -C(=Y)-NR6R7 radical; Y represents NR8, O or S; Z represents NR9, O or S; R1 and R2, independently of one another, denote hydrogen or one or more substituents other than hydrogen; the radicals R3, R4, R6, R8 and R9 independently of one another denote hydrogen or lower alkyl; and R5 and R7 independently of one another represent hydrogen, lower alkyl, hydroxyl, etherified or esterified hydroxyl or unsubstituted or mono- or disubstituted amino; tautomers thereof, and salts thereof. They have useful pharmaceutical properties and are particularly active against tumours. They are prepared in a manner known per se.

Indan-1,3-Dion und Indan-1,2,3-Trionderivate, Verfahren zu ihrer Herstellung und ihre therapeutische Verwendung

Metal complexes and methods of treatment

In one embodiment, the present application discloses compounds that are selective neuroactive agents for the treatment of diseases of the central nervous system (CNS). In one aspect, the neuroactive agents are NCDs of metal chelates, including complexes of iron, copper or zinc.

ARYLHYDRAZONES

Cytotoxic compounds

The present invention relates to a compound of general formula (I) or a pharmaceutically acceptable salt or solvate or thereof. In particular, the present invention relates to a method treating diseases involving cell proliferation, migration, apoptosis, or adhesion, comprising administering to a human or non-human mammalian patient an effective amount of a compound of general formula (I) or a pharmaceutically acceptable salt or solvate or thereof.

Compositions and Methods for Inhibition of Cathepsins

This invention is directed to compound of Formula I and methods of using these compounds in the treatment of conditions in which modulation of a cathepsin, particularly cathepsin K or cathepsin L, will be therapeutically useful. 2. The compound of claim 1 , wherein X is C(═O) or CH(OR).3. The compound of claim 2 , wherein X is C(═O).4. The compound of claim 1 , wherein m is zero.5. The compound of claim 4 , wherein n is zero and p is zero.6. The compound of claim 1 , wherein n is zero and p is zero.7. The compound of wherein m is 1.8. The compound of claim 7 , wherein Ris halo or acyl.9. The compound of claim 8 , wherein Ris substituted aryl-C(O)— or unsubstituted aryl-C(O)—.10. The compound of claim 8 , wherein Ris benzoyl.11. The compound of claim 1 , whereineach of n and p, independently, is zero or one; and{'sup': 3', '5, 'each of Rand R, independently, is selected from the group consisting of hydroxyl, methyl, methoxy and fluoro.'}13. The compound of claim 12 , wherein X is C(═O).14. The compound of claim 13 , wherein each of n claim 13 , m and p claim 13 , independently claim 13 , is zero or one.15. The compound of claim 13 , wherein n is one and Ris selected from the group consisting of hydroxyl claim 13 , methyl claim 13 , methoxy claim 13 , and fluoro.16. The compound of claim 13 , wherein p is one and Ris selected from the group consisting of hydroxyl claim 13 , methyl claim 13 , methoxy and fluoro18. The compound of claim 12 , wherein X is and m is zero or one.19. The compound of claim 18 , wherein each of n and p claim 18 , independently claim 18 , is zero or one. This application claims the benefit of U.S. provisional patent application No. 61/615,097, filed on 23 Mar. 2012, which application is incorporated herein by reference in its entirety.A. FieldThe present invention relates to compounds and methods of using these compounds in the treatment of conditions in which modulation of the cathepsin, particularly cathepsin K or cathepsin L, is ...

(THIO, OXO, AND SELENO) SEMICARBAZONE COMPLEXES WITH ZINC AND THEIR USE FOR TREATING CANCER

The invention provides organic complexes of Zn of formula (I) that are useful for treating cancer, as well as compositions and kits comprising such complexes, and intermediate monomer compounds that are useful for the preparation of such complexes. 4. The complex of any one of - wherein the ratio of the number of compounds of formula (I) or ions or poly-ions thereof to zinc Zn ions is about 2:1; or a solvate thereof.8. A pharmaceutical composition , comprising a complex of any one of - or a solvate thereof , and a pharmaceutically acceptable carrier.9. An injectable pharmaceutical formulation comprising , a complex of any one of - or a solvate thereof , and a pharmaceutically acceptable carrier.10. A method of inhibiting cancer cell growth in vivo or in vitro , comprising contacting a cancer cell with a complex of any one of - or a solvate thereof.11. A method of treating cancer in an animal comprising administering a complex of any one of - or a solvate thereof to the animal.12. The method of claim 11 , further comprising administering zinc to the animal.13. The method of any one of - claim 11 , wherein the cancer is caused by mutations affecting zinc binding proteins.14. The method of any one of - claim 11 , wherein the cancer is associated with a zinc binding p53 mutation.15. The method of any one of - claim 11 , wherein the cancer is associated with a zinc binding p53 mutation selected from R175 claim 11 , C176 claim 11 , H179 claim 11 , C238 claim 11 , C242 claim 11 , and G245.16. A complex of any one of - or a solvate thereof for use in medical treatment.17. A complex of any one of - or a solvate thereof for the prophylactic or therapeutic treatment of cancer.18. The complex or solvate of wherein the cancer is caused by mutations affecting zinc binding proteins.19. The complex or solvate of claim 17 , wherein the cancer is associated with a zinc binding p53 mutation.20. The complex or solvate of claim 17 , wherein the cancer is associated with a zinc binding ...

(THIO, OXO, AND SELENO) SEMICARBAZONE DERIVATIVES AND THEIR USE FOR TREATING CANCER

The invention provides compounds of formula I and II and salts thereof, wherein R, R, Y, R, and Rhave any of the meanings described in the specification, as well as compositions comprising such compounds and salts, and methods for treating cancer using such compounds and salts. 3. A pharmaceutical composition , comprising , a compound of or or a pharmaceutically acceptable salt thereof , and a pharmaceutically acceptable carrier.4. An injectable pharmaceutical formulation comprising , a compound of or or a pharmaceutically acceptable salt thereof , and a pharmaceutically acceptable carrier.5. A method of inhibiting cancer cell growth in vivo or in vitro , comprising contacting a cancer cell with a compound of any one of - or a pharmaceutically acceptable salt thereof.6. A method of treating cancer in an animal comprising administering a compound of any one of - or a pharmaceutically acceptable salt thereof to the animal.7. The method of claim 6 , further comprising administering zinc to the animal.8. The method of any one of - claim 6 , wherein the cancer is caused by mutations affecting zinc binding proteins.9. The method of any one of - claim 6 , wherein the cancer is associated with a zinc binding p53 mutation.10. The method of any one of - claim 6 , wherein the cancer is associated with a zinc binding p53 mutation selected from R175 claim 6 , C176 claim 6 , H179 claim 6 , C238 claim 6 , C242 claim 6 , and G245.11. A compound of any one of - or a pharmaceutically acceptable salt thereof claim 6 , for use in medical treatment.12. A compound of any one of - or a pharmaceutically acceptable salt thereof claim 6 , for the prophylactic or therapeutic treatment of cancer.13. The compound or pharmaceutically acceptable salt of wherein the cancer is caused by mutations affecting zinc binding proteins.14. The compound or pharmaceutically acceptable salt of claim 13 , wherein the cancer is associated with a zinc binding p53 mutation.15. The compound or pharmaceutically ...

THIOSEMICARBAZONES INHIBITORS OF LYSOPHOSPHATIDIC ACID ACYLTRANSFERASE AND USES THEREOF

Lysophosphatidic acid acyltransferase-beta (LPAAT-β) catalyzes the production of phosphatidic acid (PA) from lysophosphatidic acid (LPA). The lipid cofactor PA contributes to the activation of c-Raf, BRAF, mTOR and PKC-ζ. LPAAT-β expression is a prognostic factor in gynecologic malignancies and is being investigated as a therapeutic target in a variety of tumor types. A class of thiosemicarbazones was identified as inhibitors of LPAAT-β from a screen of a library of small molecules. A focused library of thiosemicarbazones derivatives was prepared and led to the development of compounds which potently inhibit LPAAT-β and inhibit the growth of MiaPaCa2 human pancreatic cancer cells. 2. The compound of claim 1 , wherein Ris a Calkyl.3. The compound of claim 1 , wherein Ris propenyl.4. The compound of claim 1 , wherein Ris H.5. The compound of claim 1 , wherein Ris methyl.6. The compound of claim 1 , wherein n is 2.7. The compound of claim 1 , wherein n is 3.8. The compound of claim 1 , wherein n is 2 and each Ris chosen from F claim 1 , Cl claim 1 , Br claim 1 , and CN.9. The compound of claim 1 , wherein the compound inhibits LPAAT-β.10. A method of treating cancer in a subject claim 1 , comprising: administering a therapeutically effective amount of a compound of to a subject in need thereof.11. The method of claim 10 , wherein the cancer is pancreatic cancer.12. The method of claim 10 , wherein the compound is administered with an anti-cancer agent.13. The method of claim 10 , wherein the cancer is colon cancer.14. The method of claim 10 , wherein the subject is also administered regorafenib.15. A method of treating obesity in a subject claim 1 , comprising: administering a therapeutically effective amount of a compound of to a subject in need thereof. This invention was made with Government support under Grant No. CA131400 awarded by the National Institutes of Health. The government has certain rights in this invention.Phosphatidic acid (PA) is a cofactor required ...

Compositions and Methods for Inhibition of Cathepsins

This invention is directed to compound of Formula I and methods of using these compounds in the treatment of conditions in which modulation of a cathepsin, particularly cathepsin K or cathepsin L, will be therapeutically useful. 220-. (canceled)21. A compound selected from the group consisting of:1,4-dibenzoylbenzene (1),3-benzoyl benzophenone thiosemicarbazone (3),4-Benzoyl benzophenone thiosemicarbazone (4),3-Benzoyl benzhydrol thiosemicarbazone (6),1-(3-methylbenzoyl),3-(3-methylbenzoyl)benzene thisosemicarbazone (9),1,3-bis(2-fluoro-benzoyl)-5-bromobenzene thiosemicarbazone (11),1,3-bis-(4-fluorobenzoyl)benzene thiosemicarbazone (13),1-(4-hydroxybenzoyl)-3-(4-methoxybenzoyl)benzene thiosemicarbazone (17),1-(4-methoxybenzoyl)-3-(4-hydroxybenzoyl)benzene thiosemicarbazone (18),1-(4-hydroxybenzoyl)-3-(4-methoxybenzoyl)benzene di-thiosemicarbazone (19),1,3-bis-(4-isopropoxybenzoyl)benzene thiosemicarbazone (22),1,3-bis-(4-isopropoxybenzoyl)benzene dithiosemicarbazone (23),1,3-bis-(4-bromobenzoyl)benzene thiosemicarbazone (24),1,3,5-Tribenzoyl benzene thiosemicarbazone (25),2-[(3-benzoylphenyl)(phenyl)methylene]-N-methylhydrazinecarbothioamide (27),2-[(3-benzoylphenyl)(phenyl)methylene]-1-methylhydrazinecarbothioamide (28), and1,3-bis-(4-methoxybenzoyl)benzene dithiosemicarbazone (33). This application claims the benefit of U.S. provisional patent application No. 61/615,097, filed on 23 Mar. 2012, which application is incorporated herein by reference in its entirety.A. FieldThe present invention relates to compounds and methods of using these compounds in the treatment of conditions in which modulation of the cathepsin, particularly cathepsin K or cathepsin L, is therapeutically useful.B. BackgroundThere are five classes of proteases including matrix metalloproteases (MMPs), cysteine proteases, serine proteases, aspartic proteases, and threonine proteases which catalyze the hydrolysis of peptide bonds. Due to their function in many disease states, including cancer ...

COMPOUNDS AND METHODS OF TREATING INFECTIONS

The invention provides compounds of Formula I, and methods of treating or preventing a bacterial infection in a subject using a compound of Formula I. The invention also provides the use of a compound of Formula I in the manufacture of a medicament for the treatment of a bacterial infection in a subject. The invention further provides a medical device when used in a method of treating or preventing a bacterial infection in a subject and to a medical device comprising the composition of the invention. 148.-. (canceled)49. A compound selected from the group consisting of:NCL178 4,6-bis(2-((E)-1-(4-chlorophenyl)ethylidene)hydrazinyl)pyrimidineNCL179 4,6-bis(2-((E)-4-chlorobenzylidene)hydrazinyl)pyrimidin-2-amineNCL180 (2Z,2′Z)-2,2′-(pyrimidine-4,6-diylbis(hydrazin-2-yl-1-ylidene))bis(2-(4-chlorophenyl)ethan-1-ol)NCL 181 4,6-bis(2-((E)-4-chlorobenzylidene)hydrazinyl)pyrimidineNCL183 N4,N6-bis(1-phenylethyl)pyrimidine-4,6-diamineNCL184 N4,N6-bis(1-phenylethyl)pyrimidine-2,4,6-triamineNCL185 4,6-bis(2-((E)-1-(4-chlorophenyl)ethylidene)hydrazinyl)pyrimidinehydrochlorideNCL 187 4,6-bis(2-((E)-4-chlorobenzylidene)hydrazinyl)pyrimidinehydrochlorideNCL189 (2Z,2′Z)-2,2′-(pyrimidine-4,6-diylbis(hydrazin-2-yl-1-ylidene))bis(2-(4-chlorophenyl)ethan-1-ol)hydrochlorideNCL193 4,6-bis(2-((E)-4-bromobenzylidene)hydrazinyl)pyrimidin-2-amineNCL194 N′,N′″-(2-aminopyrimidine-4,6-diyl)di(benzohydrazide)NCL195 4,6-bis(2-((E)-4-methylbenzylidene)hydrazinyl)pyrimidin-2-amineNCL 196 4,4′-((1E,1′E)-((2-aminopyrimidine-4,6-diyl)bis(hydrazin-2-yl-1-ylidene))bis(methanylylidene))diphenolNCL197 3,3′-((1E,1′E)-((2-aminopyrimidine-4,6-diyl)bis(hydrazin-2-yl-1-ylidene))bis(methanylylidene))diphenolNCL198 4,6-bis(2-((E)-4-(tert-butyl)benzylidene)hydrazinyl)pyrimidin-2-aminedihydrochlorideNCL199 4,6-bis(2-((E)-benzylidene)hydrazinyl)pyrimidin-2-amineNCL200 4,6-bis(2-((E)-4-(tert-butyl)benzylidene)hydrazinyl)pyrimidin-2-amineNCL201 4,4′-((1E,1′E)-((2-aminopyrimidine-4,6-diyl)bis(hydrazin-2-yl-1-ylidene)) ...

COMPOSITIONS AND METHODS FOR NON-INVASIVE IMAGING

The present invention relates to a novel composition useful in targeted diagnostic and/or therapy of a target site, such as cancerous tissue. The composition and methods disclosed herein find particular use in diagnosing and imaging cancerous tissue. The present invention provides a new diagnostic tool for the utilization of positron emission tomography (PET) imaging technique. 146-. (canceled)49. A composition comprising:(a) liposomes in a pharmaceutically acceptable medium, said liposomes each having an interior space and a membrane separating said interior space from said medium, said membrane comprising one or more lipids; and{'claim-ref': {'@idref': 'CLM-00047', 'claim 47'}, '(b) a compound of entrapped in at least one liposome of the liposomes of (a).'}50. A composition comprising:(a) liposomes in a pharmaceutically acceptable medium, said liposomes each having an interior space and a membrane separating said interior space from said medium, said membrane comprising one or more lipids; and{'claim-ref': {'@idref': 'CLM-00048', 'claim 48'}, '(b) a compound of entrapped in at least one liposome of the liposomes of (a).'}52. The composition claim 48 , wherein M is d) and the composition comprises at least 0.1 μCi of a radioisotope of copper.53. The composition claim 49 , wherein claim 49 , following storage at a temperature of from 4° C. to 40° C. or a room temperature of about 25° C. or is 37° C. for 90 days claim 49 , or 4 months claim 49 , or 5 months claim 49 , or 6 months claim 49 , less than 15% of the compound has degraded.55. The method of claim 54 , wherein prior to becoming encapsulated by the at least one liposome claim 54 , the compound of Formula III is uncharged claim 54 , and subsequent to becoming encapsulated by at least one liposome claim 54 , the compound of Formula III is charged.56. A method of imaging a tissue in a patient claim 54 , the method comprising:{'claim-ref': {'@idref': 'CLM-00048', 'claim 48'}, '(a) injecting the patient with a ...

Compositions and Methods for Non-Invasive Imaging

The present invention relates to a novel composition useful in targeted diagnostic and/or therapy of a target site, such as cancerous tissue. The composition and methods disclosed herein find particular use in diagnosing and imaging cancerous tissue. The present invention provides a new diagnostic tool for the utilization of positron emission tomography (PET) imaging technique. 133-. (canceled)35. The method of wherein background is determined by scanning tumor-free muscle tissue within 48 hours following the injection.36. The method of claim 34 , wherein claim 34 , if the image shows that the liposomal imaging agent is deposited in the tumor at levels higher than background claim 34 , then the patient is treated with the liposomal therapeutic agent and if the image shows that the liposomal imaging agent is not deposited in the tumor at levels higher than background claim 34 , then the patient is not treated with the liposomal therapeutic agent.3746-. (canceled)47. The method according to claim 34 , further comprising administering a liposomal therapeutic agent to the patient after detecting the liposomal imaging agent in the patient.48. The method of claim 47 , wherein the liposomal therapeutic agent is a liposomal antineoplastic therapeutic agent.49. The method of claim 48 , wherein the liposomal therapeutic agent is a liposomal irinotecan or liposomal doxorubicin.50. The method of claim 34 , wherein the patient is diagnosed with a neoplasia prior to injection of the liposomal imaging agent.51. The method of claim 50 , wherein the neoplasias is selected from the group consisting of fibrosarcoma claim 50 , myxosarcoma claim 50 , liposarcoma claim 50 , chondrosarcoma claim 50 , osteogenic sarcoma claim 50 , chordoma claim 50 , angiosarcoma claim 50 , endotheliosarcoma claim 50 , lymphangiosarcoma claim 50 , lymphangioendotheliosarcoma claim 50 , synovioma claim 50 , mesothelioma claim 50 , Ewing's tumor claim 50 , leiomyosarcoma claim 50 , rhabdomyosarcoma claim 50 ...

REDOX-DIRECTED CHELATORS TARGETING INTRACELLULAR METAL IONS

The present invention provides redox-activated chelators and methods for using the same to treat cancer. In one particular embodiment, the redox-activated chelator is of the formula: 1. A method for treating a clinical condition associated with a metal ion dysregulation in a subject in need of such a treatment , said method comprising administering to the subject a therapeutically effective amount of a redox-activated pro-chelator , wherein said redox-activated pro-chelator is preferentially reduced within a cell having a metal ion dysregulation to produce a metal ion chelating moiety whereby chelation of metal ion by said metal ion chelating moiety within the cell with a metal dysregulation alleviates said clinical condition associated with the metal dysregulation.2. The method of claim 1 , wherein said metal ion chelating moiety comprises a thiosemicarbazone moiety.3. The method of claim 1 , wherein said redox-activated pro-chelator comprises a disulfide linkage that is configured to selectively be reduced within a cancer cell to produce a thiol compound that is configured to chelate iron ion within the cancer cell.5. The method of claim 4 , wherein m and n are 0.6. The method of claim 4 , wherein each of Rand Ris independently hydrogen claim 4 , methyl or phenyl.10. The method of claim 9 , wherein said clinical condition comprises cancer claim 9 , a neurodegenerative disorder claim 9 , hemochromatosis claim 9 , or thalassemia.11. The method of claim 10 , wherein said clinical condition comprises breast cancer claim 10 , lung cancer claim 10 , prostate cancer claim 10 , leukemia or ovarian cancer. This application claims the priority benefit of U.S. Provisional Application No. 61/899,262, filed Nov. 3, 2013, which is incorporated herein by reference in its entirety.The present invention relates to redox-activated chelators and methods for using the same to treat cancer.It is believed that compared to normal cells, cancer cells require higher iron levels in order ...

PESTICIDALLY ACTIVE OXIME AND HYDRAZONE DERIVATIVES

The present invention relates to compounds of formula (I) as defined herein, to processes for preparing them, to pesticidal, in particular insecticidal, acaricidal, molluscicidal and nematicidal compositions comprising them and to methods of using them to combat and control pests such as insect, acarine, mollusc and nematode pests. 2. A compound according to claim 1 , wherein Arand Arare independently of each other phenyl claim 1 , thienyl claim 1 , pyridyl claim 1 , pyrimidinyl claim 1 , pyrazinyl claim 1 , pyridazinyl claim 1 , furanyl claim 1 , wherein said phenyl claim 1 , thienyl claim 1 , pyridyl claim 1 , pyrimidinyl claim 1 , pyrazinyl claim 1 , pyridazinyl claim 1 , furanyl is unsubstituted or substituted by one to three substituents independently selected from C-Calkyl claim 1 , C-Calkenyl claim 1 , C-Calkynyl claim 1 , CcycloalkylCalkyl claim 1 , C-Chaloalkyl claim 1 , C-Chaloalkenyl claim 1 , C-Chaloalkynyl claim 1 , ChalocycloalkylCalkyl claim 1 , C-Chaloalkyl-C-Ccycloalkyl claim 1 , heterocyclylCalkyl claim 1 , halogen claim 1 , cyano claim 1 , cyano-C-Calkyl claim 1 , cyano-C-Ccycloalkyl claim 1 , nitro claim 1 , C-Calkoxy claim 1 , C-Chaloalkoxy claim 1 , C-Calkoxy-C-Calkyl claim 1 , —S—C-Calkyl claim 1 , —S(O)—C-Calkyl claim 1 , —S(═O)C-Calkyl claim 1 , —S(═O)(═NH)C-Calkyl claim 1 , C-Calkylamino claim 1 , C-Cdialkylamino claim 1 , C-Ccycloalkylamino claim 1 , C-Calkyl-C-Ccycloalkylamino claim 1 , C-Calkylcarbonyl claim 1 , CHO claim 1 , C-Calkoxycarbonyl claim 1 , C-Chaloalkoxycarbonyl claim 1 , C-Calkylaminocarbonyl claim 1 , C-Chaloalkylaminocarbonyl or C-Cdialkylaminocarbonyl.3. A compound according to claim 1 , wherein Aris phenyl which is unsubstituted or substituted by one to three substituents independently selected from C-Calkyl claim 1 , C-Calkenyl claim 1 , C-Calkynyl claim 1 , C-Ccycloalkyl claim 1 , C-Chaloalkyl claim 1 , C-Chalocycloalkyl claim 1 , C-Chaloalkyl-C-Ccycloalkyl claim 1 , heterocyclylCalkyl claim 1 , halogen claim 1 , ...

(THIO, OXO AND SELENO) SEMICARBAZONE COMPLEXES WITH ZINC AND THEIR USE FOR TREATING CANCER

The invention provides organic complexes of Zn that are useful for treating cancer, as well as compositions and kits comprising such complexes, and intermediate monomer compounds that are useful for the preparation of such complexes. 3. (canceled)4. The complex of claim 1 , wherein the ratio of the number of compounds of formula (I) or ions or poly-ions thereof; or solvates thereof to zinc Zn ions is about 2:1; or a solvate thereof.57-. (canceled)8. A pharmaceutical composition claim 1 , comprising a complex of claim 1 , or a solvate thereof claim 1 , and a pharmaceutically acceptable carrier.9. An injectable pharmaceutical formulation comprising claim 1 , a complex of claim 1 , or a solvate thereof claim 1 , and a pharmaceutically acceptable carrier.1024-. (canceled)26. The complex or of claim 1 , wherein Ris selected from (C-C)alkyl claim 1 , aryl claim 1 , and aryl(C-C)alkyl; or a solvate thereof.27. The complex of claim 1 , wherein Rand each Rare each independently selected from (C-C)alkyl claim 1 , aryl claim 1 , and aryl(C-C)alkyl; or a solvate thereof. This application is a Continuation application of U.S. application Ser. No. 15/545,966, filed Jul. 24, 2017, which is a 35 U.S.C. § 371 application of International Application No. PCT/US2016/015183, filed Jan. 27, 2016, which claims the benefit of priority to U.S. Provisional Nos. 62/258,177, filed Nov. 20, 2015 and 62/108,415, filed Jan. 27, 2015, each of which is incorporated by referenced in its entirety.The disclosure relates to organic complexes of zinc and their use in the treatment of cancer.TP53 is the most commonly mutated gene in human cancer for which no effective targeted anti-cancer drug exists. The majority of TP53 mutations (>70%) are mis-sense mutations that generate a defective protein that is generally found at high levels in cancer cells due to loss of MDM2 negative feedback. Restoring the function of p53 in mouse models of cancer is highly therapeutic. Reactivating mutant p53 using small ...

SMALL MOLECULES FOR THE MODULATION OF MCL-1 AND METHODS OF MODULATING CELL DEATH, CELL DIVISION, CELL DIFFERENTIATION AND METHODS OF TREATING DISORDERS

This invention relates to compounds which selectively bind to the survival protein MCL-1 with high affinity and selectivity, pharmaceutical compositions containing such compounds and the use of those compounds or compositions for modulating MCL-1 activity and for treating hyperproliferative disorders, angiogenesis disorders, cell cycle regulation disorders, autophagy regulation disorders, inflammatory disorders, and/or infectious disorders and/or for enhancing cellular engraftment and/or wound repair, as a sole agent or in combination with other active ingredients. 136-. (canceled)38. The compound of claim 37 , wherein n is 0.39. The compound of claim 37 , wherein q is 0.40. The compound of claim 37 , wherein X is ═O.41. The compound of claim 37 , wherein Ris —SO—R claim 37 , in which Ris substituted aryl.42. The compound of claim 41 , wherein Ris 4-methylphenyl.43. The compound of claim 37 , wherein Ris —S—Rin which Ris unsubstituted heteroaryl.44. The compound of claim 43 , wherein Ris 1 claim 43 ,2 claim 43 ,4-triazolyl.46. A pharmaceutical composition comprising the compound of or a physiologically acceptable salt claim 37 , solvate claim 37 , hydrate or stereoisomer thereof and a pharmaceutically acceptable diluent or carrier.47. A method of selectively modulating MCL-1 in a cell claim 37 , comprising contacting the cell with one or more compounds of claim 37 , thereby regulating MCL-1 in the cell.48. A method for modulating apoptotic cell death in a cell claim 37 , comprising contacting the cell with one or more compounds of claim 37 , thereby regulating apoptotic cell death in the cell.49. A method for modulating autophagy in a cell claim 37 , comprising contacting the cell with one or more compounds of claim 37 , thereby regulating autophagy in the cell.50. A method for modulating necrotic cell death in a cell claim 37 , comprising contacting the cell with one or more compounds of claim 37 , thereby regulating necrotic cell death in the cell.51. A method for ...

SMALL MOLECULES FOR THE MODULATION OF MCL-1 AND METHODS OF MODULATING CELL DEATH, CELL DIVISION, CELL DIFFERENTIATION AND METHODS OF TREATING DISORDERS

This invention relates to compounds which selectively bind to the survival protein MCL-1 with high affinity and selectivity, pharmaceutical compositions containing such compounds and the use of those compounds or compositions for modulating MCL-1 activity and for treating hyperproliferative disorders, angiogenesis disorders, cell cycle regulation disorders, autophagy regulation disorders, inflammatory disorders, and/or infectious disorders and/or for enhancing cellular engraftment and/or wound repair, as a sole agent or in combination with other active ingredients. 25.-. (canceled)6. A pharmaceutical composition comprising a compound according to or a physiologically acceptable salt claim 1 , solvate claim 1 , hydrate or stereoisomer thereof and a pharmaceutically acceptable diluent or carrier.710.-. (canceled)11. A method of selectively modulating MCL-1 in cells comprising contacting a cell with one or more compounds of claim 1 , thereby regulating MCL-1 in said cell.12. A method for modulating apoptotic cell death in a cell comprising contacting a cell with one or more compounds of claim 1 , thereby regulating apoptotic cell death in said cell.13. A method for modulating autophagy in a cell comprising contacting a cell with one or more compounds of claim 1 , thereby regulating autophagy in said cell.14. A method for modulating necrotic cell death in a cell comprising contacting a cell with one or more compounds of claim 1 , thereby regulating necrotic cell death in said cell.15. A method for modulating metabolism in a cell comprising contacting a cell with one or more compounds of claim 1 , thereby regulating energy production and consumption to effect cell viability in said cell.16. A method for modulating cell division in a cell comprising contacting a cell with one or more compounds of claim 1 , thereby regulating proliferation in said cell.17. A method for modulating transcription in a cell comprising contacting a cell with one or more compounds of claim 1 , ...

COMPOSITIONS AND METHODS FOR INHIBITION OF CATHEPSINS

This invention is directed to compound of Formula I and methods of using these compounds in the treatment of conditions in which modulation of a cathepsin, particularly cathepsin K or cathepsin L, will be therapeutically useful. 2. The method of claim 1 , wherein the cathepsin is cathepsin K or cathepsin L.3. The method of claim 1 , further comprising: contacting the cathepsin in vitro with the compound having formula I.4. The method of claim 1 , further comprising contacting the cathepsin in a cell with the compound having formula I.5. The method of claim 1 , wherein X is C(═O) or CH(OR).6. The method of claim 5 , wherein X is C(═O).7. The method of claim 1 , wherein m is zero.8. The method of claim 7 , wherein n is zero and p is zero.9. The method of claim 1 , wherein n is zero and p is zero.10. The method of claim 1 , wherein m is 1.11. The method of claim 10 , wherein Ris halo or acyl.12. The method of claim 11 , wherein Ris substituted aryl-C(O)—or unsubstituted aryl-C(O)—.13. The method of claim 11 , wherein Ris benzoyl.14. The method of claim 1 , whereineach of n and p, independently, is zero or one; and{'sup': 3', '5, 'each of Rand R, independently, is selected from the group consisting of hydroxyl, methyl, methoxy and fluoro.'}16. The method of claim 5 , wherein X is C(═O).17. The method of claim 16 , wherein each of n claim 16 , m and p claim 16 , independently claim 16 , is zero or one.18. The method of claim 16 , wherein n is one and Ris selected from the group consisting of hydroxyl claim 16 , methyl claim 16 , methoxy claim 16 , and fluoro.19. The method of claim 16 , wherein p is one and Ris selected from the group consisting of hydroxyl claim 16 , methyl claim 16 , methoxy and fluoro20. The method of claim 16 , wherein m is one and Ris selected from the group consisting of halo and acyl.22. A compound of claim 21 , wherein each of n and p claim 21 , independently claim 21 , is zero or one.24. The method of claim 15 , wherein n=1 claim 15 , m=0 claim ...

Способы лечения протозойных инфекций

РОССИЙСКАЯ ФЕДЕРАЦИЯ (19) RU (11) (13) 2017 109 719 A (51) МПК A61K 31/155 (2006.01) ФЕДЕРАЛЬНАЯ СЛУЖБА ПО ИНТЕЛЛЕКТУАЛЬНОЙ СОБСТВЕННОСТИ (12) ЗАЯВКА НА ИЗОБРЕТЕНИЕ (21)(22) Заявка: 2017109719, 28.08.2015 (71) Заявитель(и): НЕОКЬЮЛИ ПТИ ЛТД (AU) Приоритет(ы): (30) Конвенционный приоритет: 02.09.2014 AU 2014903503 28 (85) Дата начала рассмотрения заявки PCT на национальной фазе: 03.04.2017 AU 2015/000527 (28.08.2015) (87) Публикация заявки PCT: A WO 2016/033635 (10.03.2016) Адрес для переписки: 191002, Санкт-Петербург, а/я 5, Общество с ограниченной ответственностью "Ляпунов и партнеры" R U (57) Формула изобретения 1. Способ лечения или предупреждения протозойной колонизации или инфекции у субъекта, включающий стадию, в которой субъекту вводят терапевтически эффективное количество соединения Формулы I или его стереоизомера, таутомера, фармацевтически приемлемой соли или пролекарства, при этом протозойная инфекция вызвана протозойным агентом, где Формула I представляет собой: где R1 представляет собой Н, циклоалкил, Формулу II или Формулу III; Стр.: 1 A 2 0 1 7 1 0 9 7 1 9 (54) СПОСОБЫ ЛЕЧЕНИЯ ПРОТОЗОЙНЫХ ИНФЕКЦИЙ 2 0 1 7 1 0 9 7 1 9 (86) Заявка PCT: R U (43) Дата публикации заявки: 04.10.2018 Бюл. № (72) Автор(ы): ПЭЙДЖ Стефен (AU), СТИВЕНС Эндрю (AU), МАККЛАСКИ Адам (AU), КИНАН Мартина (AU), АБРАХАМ Ребекка (AU) где R3 выбран из группы, состоящей из: Н; NH2; NHNH2; O-СН2-СН3; NH-C(O)-фенила; NH-CH-хлорфенила; NH-хлорфенила; NH-CH2-хлорфенила; NH-N-СН-циклоалкила; N и R4 представляет собой CH-N-CH-CCl- и R4 связан с R3; Формулы IV; Формулы V; и Формулы VI; R U R U 2 0 1 7 1 0 9 7 1 9 A Стр.: 2 A A2 представляет собой N, С, NH, N-C(O)-фенил или Формулу VII, или (СН2)n, где n равен целому числу от 1 до 3, включительно; где A3, A4, A5, A6, A7, A8, A11, A12, A13, A14, A15, A16, A17, A18, A19, A20, A21 A23, A24, A25, A26 и A27 независимо представляют собой С, О, N, NH, S; где А9 представляет собой С, О, N, NH, N-C(O)-O-CH2-CH3, N-C(O)-O-СН(СН3)2, NC(O)-NH-CH2-CH3, N-C(O ...

Антинеоплазические соединения и фармацевтические композиции на их основе

1. Химические соединения, блокирующие опосредованное казеин-киназой 2 (СК2) фосфорилирование, характеризующиеся выполнением любого или нескольких из следующих требований: ! а. связывание с фосфороакцепторным участком субстрата, тем самым блокируя прямым или косвенным образом связывание фермента СК2 с субстратом; ! b. блокирование прямым или косвенным образом переноса фосфатной группы к фосфороакцептору серина; ! c. связывание с субстратным белком СК2, вызывающее конформационное изменение в домене фосфорилирования, его окружении или в их обоих, прямым или косвенным образом выполняя действия по п.а или п.b. ! 2. Химические соединения и их гомологические варианты по п.1, в которых химическая структура определяется присутствием в любой части молекулы некоторых химических элементов, связанных упорядоченным образом с указанной электронной гибридизацией и выбранных, по крайней мере, из одной из следующих пяти структурных групп: ! I. N-[C(sp2)]1,2,3-N; ! II. N-[C(sp2)]1,2,-[C(sp3)]1,2,3-N; ! III. N-[C(sp3)]1,2,3-N; ! IV. N-C(sp2)-[C(sp3)]1,2-C(sp2)-N; ! V. N-C(sp3)-[C(sp2)]1,2-C(sp3)-N. ! 3. Фармацевтическая композиция для лечения заболеваний или состояний, в отношении которых фермент СК2 может играть патологическую роль и/или других, относящихся к неоплазическим процессам, включающая одно или более химических соединений и/или их фармацевтически приемлемых солей, как определено в пп.1 и 2, в сочетании с другими фармацевтически приемлемыми носителями или добавками. ! 4. Применение химических соединений, как определено в любом из п.1 или 2, для приготовления лекарственных средств для ингибирования пролиферации опухолевых клеток in vitro, in vivo или в связанных с организмом человека системах, для лечен� РОССИЙСКАЯ ФЕДЕРАЦИЯ (19) RU (11) 2007 146 169 (13) A (51) МПК C07F 9/22 (2006.01) ФЕДЕРАЛЬНАЯ СЛУЖБА ПО ИНТЕЛЛЕКТУАЛЬНОЙ СОБСТВЕННОСТИ, ПАТЕНТАМ И ТОВАРНЫМ ЗНАКАМ (12) ЗАЯВКА НА ИЗОБРЕТЕНИЕ (21), (22) Заявка: 2007146169/04, 05.05.2006 (71) Заявитель(и): СЕНТРО ДЕ ИНЖЕНЬЕРИА ...

Pyridyl alkylguanidine compounds, composition therewith, and methods of inhibiting H-2 histamine receptors

The compounds are pyridyl alkylguanidines, for example N-benzenesulphonyl-N'-methyl-N"-[2-((3-hydroxy-2-pyridyl)methylthio)ethyl]guanidine, which are inhibitors of histamine activity.

Patent RU2017109719A3

7 ВУ"? 2017109719” АЗ Дата публикации: 18.01.2019 Форма № 18 ИЗИМ-2011 Федеральная служба по интеллектуальной собственности Федеральное государственное бюджетное учреждение Я «Федеральный институт промышленной собственности» (ФИПС) ОТЧЕТ О ПОИСКЕ 1. . ИДЕНТИФИКАЦИЯ ЗАЯВКИ Регистрационный номер Дата подачи 2017109719/04(017045) 28.08.2015 РСТ/АО2015/00052/7 28.08.2015 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. 2014903503 02.09.2014 АО Название изобретения (полезной модели): [Х] - как заявлено; [ ] - уточненное (см. Примечания) СПОСОБЫ ЛЕЧЕНИЯ ПРОТОЗОЙНЫХ ИНФЕКЦИЙ Заявитель: НЕЁОКЬЮЛИ ПТИ ЛТД, АЧ 2. ЕДИНСТВО ИЗОБРЕТЕНИЯ [Х] соблюдено [ ] не соблюдено. Пояснения: см. Примечания 3. ФОРМУЛА ИЗОБРЕТЕНИЯ: [Х] приняты во внимание все пункты мп 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) Аб/1К 31/155 (2006.01) Аб1Р 33/02 (2006.01) 5. ОБЛАСТЬ ПОИСКА 5.1 Проверенный минимум документации РСТ (указывается индексами МПК) Аб1К 31/155 Аб1Р 33/02 5.2 Другая проверенная документация в той мере, в какой она включена в поисковые подборки: 5.3 Электронные базы данных, использованные при поиске (название базы, и если, возможно, поисковые термины): Езрасепе, Соозе, Соо]е Ржеп$, РАТЕМТСОРЕ, Раб Срет, Ри Мед, Кеахуз, эслепсе Оиесё Уап4ех 6. ДОКУМЕНТЫ, ОТНОСЯЩИЕСЯ К ПРЕДМЕТУ ПОИСКА Кате- Наименование документа с указанием (где необходимо) частей, Относится к гория* относящихся к ...

Thioether compounds as nitrification inhibitors

Provided herein are a use of thioether compounds of formula I as nitrification inhibitors, and agricultural mixtures and compositions including the thioether compounds.

CATECHOLHYDRAZONE DERIVATIVES, METHOD FOR THE PRODUCTION THEREOF AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM

METHODS FOR TREATING PROTOZOIC INFECTIONS

РОССИЙСКАЯ ФЕДЕРАЦИЯ (19) RU (11) (13) 2020 113 652 A (51) МПК A61K 31/155 (2006.01) ФЕДЕРАЛЬНАЯ СЛУЖБА ПО ИНТЕЛЛЕКТУАЛЬНОЙ СОБСТВЕННОСТИ (12) ЗАЯВКА НА ИЗОБРЕТЕНИЕ (21)(22) Заявка: 2020113652, 28.08.2015 (71) Заявитель(и): НЕОКЬЮЛИ ПТИ ЛТД (AU) Приоритет(ы): (30) Конвенционный приоритет: (43) Дата публикации заявки: 10.06.2020 Бюл. № 16 (72) Автор(ы): ПЭЙДЖ Стефен (AU), СТИВЕНС Эндрю (AU), МАККЛАСКИ Адам (AU), КИНАН Мартина (AU), АБРАХАМ Ребекка (AU) R U (57) Формула изобретения 1. Способ лечения или предупреждения протозойной колонизации или инфекции у субъекта, включающий стадию введения терапевтически эффективного количества соединения или его фармацевтически приемлемой соли, выбранного из группы, состоящей из: 4,6-бис(2((E)-1-(4-хлорфенил)этилиден)гидразинил)пиримидина (NCL178); 4,6-бис(2((E)-4-хлорбензилиден)гидразинил)пиримидин-2-амина (NCL179); (2Z,2'Z)-2,2'-(пиримидин-4,6-диилбис(гидразин-2-ил-1-илиден))бис(2-(4-хлорфенил) этан-1-ола) (NCL180); 4,6-бис(2-((E)-4-хлорбензилиден)гидразинил)пиримидина (NCL181); 6-хлор-N4-(1-фенилэтил)пиримидин-2,4-диамина (NCL182); N4,N6-бис(1-фенилэтил)пиримидин-4,6-диамина (NCL183); N4,N6-бис(1-фенилэтил)пиримидин-2,4,6-триамина (NCL184); 4,6-бис(2-((E)-1-(4-хлорфенил)этилиден)гидразинил)пиримидин гидрохлорида (NCL185); 4,6-бис(2-((E)-4-хлорбензилиден)гидразинил)пиримидин гидрохлорида (NCL187); (2Z,2'Z)-2,2'-(пиримидин-4,6-диилбис(гидразин-2-ил-1-илиден))бис(2-(4-хлорфенил) этан-1-ол) гидрохлорида (NCL189); 4,6-бис(2-((E)-4-бромбензилиден)гидразинил)пиримидин-2-амина (NCL193); N',N'''-(2-аминопиримидин-4,6-диил)ди(бензoгидрaзида) (NCL194); 4,6-бис(2-((E)-4-метилбензилиден)гидразинил)пиримидин-2-амина (NCL195); 4,4'-((1E,1'E)-((2-аминопиримидин-4,6-диил)бис(гидразин-2-ил-1-илиден))бис (метанилилиден))дифенола (NCL196); 3,3'-((1E,1'E)-((2-аминопиримидин-4,6-диил)бис(гидразин-2-ил-1-илиден))бис Стр.: 1 A 2 0 2 0 1 1 3 6 5 2 A (54) СПОСОБЫ ЛЕЧЕНИЯ ПРОТОЗОЙНЫХ ИНФЕКЦИЙ 2 0 2 0 1 1 3 6 5 2 Адрес для переписки: 191002, Санкт- ...

Hydrazones

일반식(I)의 화합물은 유용한 약제학적 특성을 가지며 중앙치료에 특히 효과적이다. 이들은 공지된 방법 자체로 제조된다. Compounds of formula (I) have useful pharmaceutical properties and are particularly effective for central therapy. They are prepared by known methods per se. 상기식에서, In the above formula, A 는 직접 결합이거나 -(CH 2 )n- (여기서, n은 1,2 또는 3이다) 이고 A is a direct bond or-(CH 2 ) n- where n is 1,2 or 3 X 는 라디칼 -C(=Y)-NR 6 R 7 이며; X is radical -C (= Y) -NR 6 R 7 ; Y 는 NR 8 , 산소 또는 황이고; Y is NR 8 , oxygen or sulfur; Z 는 NR 9 , 산소 또는 황이며; Z is NR 9 , oxygen or sulfur; R 1 및 R 2 는 각각 독립적으로 수소 또는 수소 이외의 R 1 and R 2 are each independently hydrogen or other than hydrogen 하나 이상의 치환체이고; One or more substituents; 라디칼 R 3 , R 4 , 4 6 , R 8 및 R 9 는 각각 독립적으로 수소 또는 저급 알킬이며; The radicals R 3 , R 4 , 4 6 , R 8 and R 9 are each independently hydrogen or lower alkyl; R 5 및 R 7 는 각각 독립적으로 수소, 저급 알킬, 하이드록시, 에테르화되거나 에스테르화된 하이드록시 또는 비치환 되거나 일- 또는 이치환된 아미노이다. R 5 and R 7 are each independently hydrogen, lower alkyl, hydroxy, etherified or esterified hydroxy or unsubstituted or mono- or disubstituted amino.

Thioether compounds as nitrification inhibitors

本发明涉及式I的硫醚化合物作为硝化抑制剂的用途以及包含所述硫醚化合物的农业混合物和组合物。

Patent RU2018131442A3

ВУ’ 2018131442” АЗ Дата публикации: 30.09.2021 Форма № 18 ИЗПМ-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 2018131442/04(051259) 31.08.2018 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. 2013901516 01.05.2013 АО Название изобретения (полезной модели): [Х] - как заявлено; [ ] - уточненное (см. Примечания) СОЕДИНЕНИЯ И СПОСОБЫ ЛЕЧЕНИЯ ИНФЕКЦИЙ Заявитель: НЕОКУЛИ ПТИ ЛТД, АЧ 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) (070 239/48 (2006.01) Аб1К 31/505 (2006.01) АО1М№М 43/68 (2006.01) (070 239/50 (2006.01) Аб1К 31/53 (2006.01) Аб1Р 31/4 (2006.01) (070 251/66 (2006.01) АО01М 43/54 (2006.01) 5. ОБЛАСТЬ ПОИСКА 5.1 Проверенный минимум документации РСТ (указывается индексами МПК) С07р 239/48, С07Р 239/50, С07О 251/66, Аб1К 31/505, Аб1К 31/53, АОЛМ 43/54, АОМ 43/68, Аб1Р 31/04 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): Езрасепе, Соозе, РАТЕМТСОРЕ, Рабеагсв, РиБСВет, Кеахуз, эГМ ...

Animal growth stimulator

Изобретение относитс  к области животноводства.Известно средство стимул ции роста животных путем взедени  в корм производных хинона, в частности хино- ксалина [1].Однако, производные хиноксалина обладают канцерогенным действием и опасны дл  здоровь  животных и людей.Целью изобретени   вл етс  усиление ростстимулирующего действи  предложенного средства при -обеспечении его безвредности дл  здоровь  человека и животных.Дл  достижени  указанной цели в корм ввод т производное хинона общей формулы где X - гуанидинимино-радикал, необ зательно содержащий 1-3 заместител  у атомов азота из числа C^,j —алкилрадикалов и фенилрадикалов, необ зательно замещенные атомами галоида, например атомами хлора; или 1,3-диазо-2-ен-гетероцикл-2-гидразо- норадикал; и У-гуанидиниминораликал,необ зательно замещенный названными заместител ми, 3-нитрогуанидинимино- радикал; семикарбазоно-или тиосеми- карбазонорадикал, необ зательно замещенный у атома N. карбамоилрадика- лом, бензилрадикалом, C^.j -алкил- или алкенилрадикалбм или фенилрадикалом; или 3-[1 ,'4-(гуанидинимино) циклогекса-2,5-диэнилиденимино)] 10 гуанидинимино- или 3- 4-семикарбазо- ноциклогекса-2,5-диэнилидениминогуа- нидиниминорадикал или его дигидропроизводное или его соль. Когда в' производном хинона формулы X или У гуанйдиниминорадикал, предпочтительно, чтобы он или не содержал заместителей, или содержал только один заместитель у атома азота, предпочтительно у концевого, и чтобы он был таким заместителем, как метил-, бензил- или карбамоилрадикал. The invention relates to the field of animal husbandry. A means of stimulating the growth of animals is known by taking quinone derivatives, in particular quinoxaline, into feed [1]. However, quinoxaline derivatives are carcinogenic and dangerous to the health of animals and humans. The purpose of the invention is to enhance the growth-stimulating effect of the proposed agent in ensuring that it is harmless to human and animal health. To achieve this goal, a quinone derivative ...

Antineoplastic compounds and pharmaceutical compositions thereof

The invention relates to chemical compounds which are obtained by means of in silico molecular modelling and which have a structure that can be used to block phosphorylation by interacting said compounds with the phosphorylation domain or the environment thereof in the substrates of the Casein Kinase II enzyme. The invention also relates to pharmaceutical compositions that contain said compounds and to the use thereof in the preparation of medicaments for the treatment of diseases associated with neoplastic processes.

Compounds and methods of treating infections

The invention provides compounds of Formula I, and methods of treating or preventing a bacterial infection in a subject using a compound of Formula I. The invention also provides the use of a compound of Formula I in the manufacture of a medicament for the treatment of a bacterial infection in a subject. The invention further provides a medical device when used in a method of treating or preventing a bacterial infection in a subject and to a medical device comprising the composition of the invention.

NOVEL TRICYCLIC COMPOUNDS, THEIR PREPARATION PROCESS, AND INTERMEDIATES THEREOF, THEIR APPLICATION AS MEDICAMENTS AND THE PHARMACEUTICAL COMPOSITIONS CONTAINING THEM

QUINON DERIVATIVE FOR USE IN AN APPROPRIATE FOR CATTLE BREEDING AND PROCEDURES FOR MANUFACTURE

Compositions used for bleeding animals

TECHNETIUM-99m COMPLEXES FOR USE AS RADIOPHARMACEUTICALS

The present invention relates to novel technetium-99m complexes and to methods of preparing the complexes. The present invention further relates to a radiopharmaceutical composition comprising the complexes, to the use of the compositions for examining the renal function, and to a kit for preparing such compositions.

Cathecol hydrazone derivatives, process for preparing the same and pharmaceutical composition containing the same

The present invention provides novel cathecol hydrazone derivatives of formula (I) or pharmaceutically acceptable salts thereof, wherein R1 is C1-7 alkyl or C3-7 cycloalkyl; R2 is hydrogen, hydroxy, C1-5 alkyl or -CH2CH2C(=O)NH2; R3 and R4 are independently hydrogen, C1-7 alkyl, -C(=X)-R5, or 2-, 3- or 4-pyridyl, prymidyl or phenyl substituted with one or two selected from a group consisting of halogen, C1-6 alkoxy, nitro, trifluoromethyl, C1-6 alkyl and carboxyl, or R3 and R4 are directly bonded by C3-4 containing oxygen, sulfur or nitrogen to form a heterocyclic ring, X is oxygen, sulfur or NH and R5 is C1-7 alkyl, -NHR6, CONH2 or 2-, 3- or 4-pyridyl, prymidyl or phenyl substituted with one selected from a group consisting of halogen, C1-6 alkoxy, nitrile, trifluoromethyl, C1-6 alkyl and carboxyl, and R6 is hydrogen, hydroxy, NH2, C1-5 alkoxy, C1-5 alkyl, pyridyl or phenyl.

Antineoplastic compounds and based pharmaceutical compositions

FIELD: medicine. ^ SUBSTANCE: invention refers to A pharmaceutical composition including of one or more compounds specified from the group given in the patent claim and having an evident cytotoxic action and an antineoplastic effect provided by their ability to block a phosphor acceptor site on casein kinase 2 substrata by direct or indirect action, as well as to application of the compounds for preparation of medical products to inhibit malignant cell proliferation. ^ EFFECT: improved clinical effectiveness. ^ 2 cl, 45 ex, 4 tbl, 1 dwg РОССИЙСКАЯ ФЕДЕРАЦИЯ (19) RU (11) 2 404 987 (51) МПК C07F C07C C07C C07C C07C C07C ФЕДЕРАЛЬНАЯ СЛУЖБА C07D ПО ИНТЕЛЛЕКТУАЛЬНОЙ СОБСТВЕННОСТИ, C07D ПАТЕНТАМ И ТОВАРНЫМ ЗНАКАМ C07D C07D (12) ОПИСАНИЕ 9/22 211/14 237/22 257/14 271/64 281/12 209/14 233/91 239/28 473/36 (24) Дата начала отсчета срока действия патента: 05.05.2006 (43) Дата публикации заявки: 20.06.2009 (56) Список документов, цитированных в отчете о поиске: GB 2673859 А, 30.03.1954. RU 2290410 С2, 27.03.2005. Silvio E. Perea et al. "Antitumor effect of a novel proapoptoic peptide that impairs the phosphorylation by the protein kinase 2'', CANCER RESEARCH 2004, 64 p.7127-7129. X., Zhao et al. "An approach to the design of molecular solids. The ureylenedicarboxylic acids", J. AM. CHEM. SOC. 1990, 112, (см. прод.) (72) Автор(ы): РОДРИГЕС ФЕРНАНДЕС Роландо Эдуардо (CU), ВЕРА АЛЬВАРЕС Роберто (CU), ДЕ ЛА НУЕС ВЕУЛЕНС Ания (CU), МАСОЛА РЕЙЕС Йулиет (CU), ПЕРЕА РОДРИГЕС Сильвио Эрнесто (CU), АСЕВЕДО КАСТРО Борис Эрнесто (CU), МУСАЧЧИО ЛАСА Алексис (CU), УБЬЕТА ГОМЕС Раймундо (CU) (73) Патентообладатель(и): СЕНТРО ДЕ ИНЖЕНЬЕРИА ГЕНЕТИКА И БИОТЕКНОЛОГИА (CU) C 2 C 2 (2006.01) (2006.01) (2006.01) (2006.01) (2006.01) (2006.01) (2006.01) (2006.01) (85) Дата перевода заявки PCT на национальную фазу: 12.12.2007 (86) Заявка PCT: CU 2006/000002 (05.05.2006) (87) Публикация PCT: WO 2006/119713 (16.11.2006) Адрес для переписки: 129090, Москва, ул.Б.Спасская, 25, стр.3, ООО "Юридическая ...

Kinase inhibitor

The present invention addresses the problem of providing: a novel kinase inhibitor and others; and a therapeutic agent for a disease, a drug discovery screening method and others, each utilizing the inhibitor and others. A compound represented by formula (I) or a salt thereof can inhibit multiple kinases including LATS (particularly LATS2) that is a major kinase involved in the Hippo signal transduction pathway, and can treat a disease or a damaged tissue both associated with cell proliferation failure. Accordingly, the present invention is useful in the field of study on cell functions, diseases and the like in which the Hippo signal transduction pathway is involved. The present invention is also useful in the medical field for treating the diseases and the like. {In the formula, each symbol is as defined in the description.}

Production of aromatic nitrile

(57)【要約】 （修正有） 【課題】 水と混和しない有機溶剤中において、第三級 アミン塩基の存在下で、対応するアルデヒドをヒドロキ シルアミンの硫酸塩と反応させることによる芳香族ニト リルの製造を提供する。 【解決手段】 式IIのアルデヒドとヒドロキシルアミン の硫酸塩とを、式III、IVまたはＶの第三級アミンの存 在下、１００乃至１６０℃の温度において、反応で遊離 する水を０．０２乃至１．５ｂａｒの範囲において留去 しながら反応させ、アンモニウム塩を除去し、常法によ って式Ｉのニトリルを単離する方法。

Intermediate for preparing tricyclic compound and preparing method thereof

本发明公开了式(I)化合物及其酸和碱加成盐和它们的酯，其中R 1 ，R 2 ，R 3 ，R 4 ，R 5 和G如说明书所定义且虚线表示任选的第二条键，本发明还公开了所述化合物的制备方法，此法的中间体，所述化合物作为药物的应用以及含有它们的药物组合物。

Antibacterial agents

본 발명은 화학식 I의 항균 화합물; 뿐만 아니라 그것의 입체 이성질체, 약학적으로 허용 가능한 염, 에스테르 및 프로드러그; 상기 화합물을 포함하는 약학 조성물; 상기 화합물의 투여에 의한 박테리아 감염의 치료 방법; 및 상기 화합물의 제조 방법을 제공한다. 화학식 I The present invention provides an antimicrobial compound of formula (I); As well as its stereoisomers, pharmaceutically acceptable salts, esters and prodrugs; Pharmaceutical compositions comprising said compounds; A method of treating bacterial infection by administration of said compound; And it provides a process for the preparation of the compound. Formula I

Metal complexes and methods of treatment

In one embodiment, the present application discloses compounds that are selective neuroactive agents for the treatment of diseases of the central nervous system (CNS). In one aspect, the neuroactive agents are NCDs of metal chelates, including complexes of iron, copper or zinc.

Tricyclic compounds having activity specific for integrins, particularly alphanubeta3 integrins, method for preparing same, intermediates therefor, use of said compounds as drugs, and pharmaceutical compositions containing same

The subject of the invention is the products of formula (I): in which R 1 , R 2 , R 3 , R 4 , R 5 and G are as defined in the description, the dotted lines represent an optional second bond, as well as the addition salts with acids and bases and the esters, their preparation process and the intermediates of this process, their use as medicines and the pharmaceutical compositions containing them.

Methods for treating protozoan infections

Compositions and methods for inhibition of cathepsins

This invention is directed to compound of Formula I and methods of using these compounds in the treatment of conditions in which modulation of a cathepsin, particularly cathepsin K or cathepsin L, will be therapeutically useful.

Antibacterial agents

METHODS AND COMPOSITIONS FOR THE BREEDING OF ANIMALS

Elevation of hdl cholesterol by 2-{(aminothioxomethyl)-hydrazono}-2-arylethyl carbamates

Compounds and methods of treating infections

The invention provides compounds of Formula (I), and methods of treating or preventing a bacterial infection in a subject using a compound of Formula (I). The invention also provides the use of a compound of Formula (I) in the manufacture of a medicament for the treatment of a bacterial infection in a subject. The invention further provides a medical device when used in a method of treating or preventing a bacterial infection in a subject and to a medical device comprising the composition of the invention.

Metal complexes and methods of treatment

在一个实施方案中，本申请公开为选择性神经活性剂的化合物，其用于治疗中枢神经系统(CNS)的疾病。在一个方面，所述神经活性剂是金属螯合物的NCD，所述金属螯合物包括铁、铜或锌的络合物。

Medicinal product based on thiosemicarbazones of unsaturated aldehydes.

Antineoplasic compounds and pharmaceuticals compositions thereof

CHEMICAL COMPOUNDS DERIVED BY IN SILICO MOLECULAR MODELING, HAVING A WELL DEFINED STRUCTURE SUITABLE FOR THE BLOCKING OF THE PHOSPHORYLATION EVENT, THROUGH THE SPECIFIC INTERACTION OF THE CHEMICAL WITH THE CASEIN KINASE 2 ENZYME SUBSTRATE PHOSPHORYLATION DOMAIN OR IT’S NEIGHBOUHOOD. THIS INVENTION COMPRISES ALSO THE PHARMACEUTICAL COMPOSITIONS CONTAINING SUCH COMPOUNDS, AND THEIR USE IN THE PREPARATION OF MEDICINES OR AGENTS FOR THE TREATMENT OF DISEASES OR CONDITIONS RELATED WITH NEOPLASIC PROCESSES.

TECHNETIUM-99m COMPLEXES FOR USE AS RADIOPHARMACEUTICALS

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

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

Tricyclic compounds having activity specific for integrins, particularly .alpha.v.beta.3 integrins, method for preparing same, intermediates therefor, use of said compounds as drugs, and pharmaceutical compositions containing same

Compounds of formula (I), wherein R¿1?, R¿2?, R¿3?, R¿4?, R¿5? and G are as defined in the description and the dotted lines indicate an optional second bond, as well as the acid, base and ester addition salts thereof, a method for preparing said compounds, intermediates therefor, the use of said compounds as drugs, and pharmaceutical compositions containing same, are disclosed.

The method for preparing thiosemicarbazide acetal

本发明公开一种制备硫代氨基脲缩醛的方法，包括步骤：a.将固态硫代氨基脲和固态芳醛类物质混合后加速，使其高速运动，相互摩擦，增强反应活性；b.在硫代氨基脲和固态芳醛运动方向上设置固定靶，高速运动的硫代氨基脲和固态芳醛撞击该固定靶，其动能转化为分子内能，分子断键活化，重新成键，合成硫代氨基脲缩醛。步骤a、b周期性循环进行，使反应充分。本方法工艺简单，流程短，使用设备少，能耗低，单次反应时间短，原料转化率大于75%，产率高，生产能力大，反应条件温和，不使用任何催化剂或溶剂，无三废排放，无需环境治理。

Antibacterial agents

Antibacterial compounds of formula I are provided: As well as stereoisomers, pharmaceutically acceptable salts, esters, and prodrugs thereof; pharmaceutical compositions comprising such compounds; methods of treating bacterial infections by the administration of such compounds; and processes for the preparation of the compounds.

Metal complexes and methods of treatment

In one embodiment, the present application discloses compounds that are selective neuroactive agents for the treatment of diseases of the central nervous system (CNS). In one aspect, the neuroactive agents are NCDs of metal chelates, including complexes of iron, copper or zinc.

S-substituted-thiosemicarbazone structure compound and preparation method and application thereof

Provided are an S-substituted-thiosemicarbazone structure compound shown in a formula I and a preparation method and an application thereof. The S-substituted-thiosemicarbazone compound shown in the formula I has an excellent prevention and treatment effect on agricultural common pathogenic bacteria, has better performance than the existing positive drug azoxystrobin in in-vitro and in-vivo tests, and has the potential of replacing or supplementing existing bactericide in the existing market.

Process for the preparation of asymmetrical bis(thiosemicarbazones)

The present invention relates to a method of making asymmetrical bis(thiosemicarbazones), compounds useful as synthetic intermediates in the method, new bis(thiosemicarbazones) that can be readily accessed by use of the method and methods of treatment and imaging utilising some of the new bis(thiosemicarbazones).

Agent for the control of ectoparasitic insect pests and their use

Bicyclic amino derivatives and pgd2 antagonist containing the same

The present invention is directed to a compound of the formula (I) wherein for example, a compound below: wherein R1 is CH3, H or Na; and X1-X2-X3 is

Metal complexes and methods of treatment

In one embodiment, the present application discloses compounds that are selective neuroactive agents for the treatment of diseases of the central nervous system (CNS). In one aspect, the neuroactive agents are NCDs of metal chelates, including complexes of iron, copper or zinc.

Antiviral methods and compositions

Disclosed herein are antiviral compounds, such as anti-human cytomegalovirus antiviral compounds, pharmaceutical compositions and antiviral methods.

Pharmacologically active compounds

Compositions and methods for non-invasive imaging

Novel thromboxane a2 antagonists

Bicyclic amino derivatives and PGD2 antagonist containing the same

A compound of the formula (I): wherein for example, a compound below: wherein R 1 is CH 3 , H or Na; and X1-X2-X3 is or its salt or a hydrate thereof is useful as PGD 2 antagonist and can be used as a drug for treating diseases in which mast cell dysfunction is involved, for example, systemic mastocytosis and disorder of systemic mast cell activation, and also tracheal contraction, asthma, allergic rhinitis, allergic conjunctivitis, urticaria, injury due to ischemic reperfusion, and as an anti-inflammatory agent. It is particularly useful in the treatment of nasal occlusion.

Inhibitors of multicatalytic protease

Compounds and Methods of Treating Infections

The invention provides compounds of Formula I, and methods of treating or preventing a bacterial infection in a subject using a compound of Formula 1. The invention also provides the use of a compound of Formula I in the manufacture of a medicament for the treatment of a bacterial infection in a subject. The invention further provides a medical device when used in a method of treating or preventing a bacterial infection in a subject and to a medical device comprising the composition of the invention.

NITROGENATED COMPOUNDS WITH ANTINEOPLASTIC ACTION AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM

Compuestos químicos nitrogenados obtenidos por modelacion molecular in silico, y cuya estructura permite el bloqueo de la fosforilacion mediante la integracion de dichos compuestos con el dominio de fosforilacion o su entorno en los sustratos de la enzima Caseína Kinasa 2. comprende además las composiciones farmacéuticas que contienen dichos compuestos y su uso en la preparacion de medicamentos para el tratamiento de enfermedades relacionadas con procesos neoplásticos. Reivindicacion 1: Compuestos químicos los cuales bloquean la fosforilacion por Caseina Kinasa 2 (CK2) y con accion antineoplástica, caracterizada porque cumple con uno o varios de los siguientes requerimientos: a) se unen al dominio de fosforilacion o a su entorno en el sustrato de la CK2, bloqueando directa o indirectamente la union de la enzima al sustrato; b) impiden directa o indirectamente la transferencia del grupo fosfato a la serina fosfoaceptora; c) su union a la proteína sustrato de la CK2, genera un cambio conformacional en el dominio de fosforilacion, su entorno a ambos, de forma directa o indirecta, acorde a los descrito en a) y b). Nitrogenous chemical compounds obtained by molecular modeling in silico, and whose structure allows the blocking of phosphorylation by integrating said compounds with the phosphorylation domain or its surroundings in the substrates of the enzyme Casein Kinase 2. It also includes pharmaceutical compositions containing said compounds and their use in the preparation of medicaments for the treatment of diseases related to neoplastic processes. Claim 1: Chemical compounds which block phosphorylation by Casein Kinase 2 (CK2) and with antineoplastic action, characterized in that it meets one or more of the following requirements: a) they bind to the phosphorylation domain or its environment in the substrate of the CK2, directly or indirectly blocking the binding of the enzyme to the substrate; b) directly or indirectly prevent the transfer of the phosphate group to ...

Hydrazone.

Agent for controlling ectoparasitic insect pests and their use

Tricyclic compounds with integrine activity, in particular towards alpha vbeta 3 intergrines, method for their preparation and use as medicamentous forms and pharmaceutical compositions containing them

Antibacterial agents

Un compuesto de acuerdo con la fórmula I:**Fórmula** o un estereoisómero, sal farmacéuticamente aceptable o éster de la misma, en el que E está ausente o está seleccionado del grupo que consiste en (1) H, (2) alquilo C1-C6 sustituido o sin sustituir, (3) arilo sustituido o sin sustituir, (4) heterociclilo sustituido o sin sustituir, y (5) heteroarilo sustituido o sin sustituir; L está ausente o está seleccionado del grupo que consiste en (1) alquilo C1-C6 sustituido o sin sustituir, (2) -(NH)0-1-(CH2)j-NR3L-(CH2)k-, (3) -(NH)0-1C(R1L, R2L)-NR3L-C(R1L, R2L)-, (4) -C(R1L, R2L)-O-C(R1L, R2L)-, (5) -(CH2)j-NR3L-C(R1L, R2L-CONH-(CH2)k-, (6) -CO-C(R1L, R2L)-NHCO-, (7) -CONH-, (8) -NHCO-, en las que R1L, R2L y R3L están seleccionados independientemente del grupo que consiste en (a) H, (b) alquilo C1-C6 sustituido o sin sustituir, (c) alquilo C1-C6 sustituido con arilo, (d) alquilo C1-C6 sustituido con heterociclilo, y (e) alquilo C1-C6 sustituido con heteroarilo, o R1L y R3L, junto con los átomos a los que están unidos, pueden formar un anillo heterocíclico sustituido o sin sustituir que tiene de 3 a 8 átomos de anillo, en el que 1-2 átomos de anillo del sistema de anillo heterocíclico están seleccionados de N, O y S; j es un número entero de 0-4; k es un número entero de 0-4; D está ausente o está seleccionado del grupo que consiste en (1) cicloalquilo C3-C8 sustituido o sin sustituir, (2) arilo sustituido o sin sustituir, (3) heterociclilo sustituido o sin sustituir, y (4) heteroarilo sustituido o sin sustituir; G está ausente o está seleccionado del grupo que consiste en (1) -C(>=O)-, (2) -C>=C-, (3) -C≡C-C≡C- and (4) -C>=C-; Y está seleccionado del grupo que consiste en (1) cicloalquilo C3-C8 sustituido o sin sustituir, (2) fenilo sustituido o sin sustituir, X está seleccionado del grupo que consiste en (1) -(C>=O)-, (2) -alquilo C1-C6-(C>=O)-, (3) -alquenilo C2-C6-C>=O)-, (4) -alquinilo C2-C6-(C>=O)-, y (5) -CH2-; B está ausente o en la que R1b y ...

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

Therapeutic compounds having the formula: ##STR1## in which R 2 and R 3 independently denote H, C 1 -C 4 alkoxy or OH and (A, B)=(oxygen, oxygen) in which case one out of R and R 1 denotes OH, halogen, secondary amino or tertiary amine and the other denotes NHNHCONHR 4 or R and R 1 together denote ═N--NH--CX--NHR 5 , ═N--NH--CX--N(phenyl) 2 , ═N--NH--CX--NH--NH--R 5 , ═N--NH--C(SCH 3 )═N--R 6 or ═N--N═C(SCH 3 )--NH--R 6 ; or (A, B)=(N--OH, oxygen) in which case R and R 1 together form ═N--NH--CX--NHR 5 or ═N--NH--CX--N(phenyl) 2 ; or (A, B)=(N--NH--CX--NHR 5 , oxygen) in which case R and R 1 together form ═N--NH--CX--NHR 5 ; or (A, B)=(N--OH, N--OH) in which case R and R 1 together form ═N--NH--CX--NHR 5 or ═N--NH--CX--N(phenyl) 2 .

Process for the preparation of pharmaceutically active arylhydrazones

Heterocyclic substituted guanidines

Process and intermediates for the preparation of triazolone derivatives

PHARMACEUTICAL PREPARATION FUNCTIONING AS PGDi2 ANTAGONIST AND BICYCLIC AMINO DERIVATIVE COMPRISED THEREIN

Bicyklická sloučenina obecného vzorce I, kde jednotlivé symboly mají specifický význam, nebo její sůl nebo hydrát, která je užitečná jako antagonist PDG.sub.2.n. a která se může použít jako léčivo pro léčbu nemocí, způsobených disfunkcí žírné buňky, například systemické mastocytózy a poruch aktivace systemické žírné buňky a také tracheální kontrakce, astmatu, alergické rinitidy, alergické konjuktivitidy, kopřivky, poranění následkem ischemické reperfůze a jako protizánětlivé činidli. Zvlášť je užitečná při léčbě nazální okluze. ŕ A bicyclic compound of formula (I) wherein the individual symbols are of particular interest, or a salt or hydrate thereof, which is useful as a PDG.sub.2 antagonist. and which can be used as a medicament for the treatment of diseases caused by mast cell dysfunction, such as systemic mastocytosis and systemic mast cell activation disorders, as well as tracheal contraction, asthma, allergic rhinitis, allergic conjunctivitis, urticaria, ischemic reperfusion injury, and anti-inflammatory agent. It is particularly useful in the treatment of nasal occlusion. ŕ

DHNB (dehydroepiandrosterone) condensed phenylthiosemicarbazide compound as well as preparation method and application thereof

本发明公开了一种化学合成药物DHNB缩苯基氨基硫脲，结构如下所示： 上述化学合成药物DHNB缩苯基氨基硫脲的制备方法，以结构式(Ⅰ)所示的3，4‑二羟基‑5‑硝基苯甲醛(DHNB)为原料，在溶剂甲醇中与结构式(Ⅱ)所示的4‑苯基氨基硫脲经醛胺进行缩合反应，合成结构式(Ⅲ)所示的DHNB缩苯基氨基硫脲；本发明通过抑制黄嘌呤氧化酶(XOD)，减少体内尿酸合成，从而有效治疗痛风和高尿酸血症。

DERIVATIVES OF INDANO-1,3-DIONA AND INDANO-1,2,3-TRIONA, THEIR PREPARATION PROCEDURES AND THEIR APPLICATION IN THERAPEUTICS.

COMPUESTOS UTILES EN TERAPEUTICA DE FORMULA (I), EN LA CUAL R2 Y R3 REPRESENTAN INDEPENDIENTEMENTE UNO DEL OTRO H, ALCOXI EN C1 NO ENTRE R Y R1 REPRESENTA OH, HALOGENO, AMINO SECUNDARIO O AMINA TERCIARIA Y EL OTRO REPRESENTA NHNHCONHR4 O BIEN R Y R1 FORMAN CONJUNTO = N = N = N A, B) = (N NH CONJUNTO = N CUYO CASO R Y R1 FORMAN CONJUNTO = N NH USEFUL COMPOUNDS IN THERAPEUTICS OF FORMULA (I), IN WHICH R2 AND R3 REPRESENT INDEPENDENTLY ONE OF THE OTHER H, ALCOXI IN C1 DOESN'T BETWEEN R AND R1 REPRESENTS OH, HALOGEN, SECONDARY AMINO OR TERTIARY AMINA4 AND NHNH REN SET = N = N = NA, B) = (N NH SET = N WHOSE CASE R AND R1 FORM SET = N NH

Methods for treating protozoan infections

The invention provides compounds of Formula (I), and their use in methods for treating or preventing a protozoan infection in a subject using a compound of Formula (I). The invention also provides the use of a compound of Formula (I) in the manufacture of a medicament for the treatment of a protozoan infection in a subject. The invention further provides a medical device when used in a method of treating or preventing a protozoan infection in a subject and to a medical device comprising the composition of the invention.