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1. 发明申请

WO2009010925A2 ANNELATED AZAHETEROCYCLIC AMIDES CONTAINING A PYRIMIDINE FRAGMENT AND METHOD FOR THE PRODUCTION AND USE THEREOF 审中-公开
标题翻译：含有吡咯烷酮片的苯胺类AZAHETEROCYICIC AMIDES及其生产和使用方法
公开(公告)号：WO2009010925A2
公开(公告)日：2009-01-22
申请号：PCT/IB2008052846
申请日：2008-07-16
申请人： ALLA CHEM LLC , IVASHCHENKO ANDREY ALEXANDROVI , IVASHCHENKO ALEXANDER VASILIEV , TKACHENKO SERGEY YEVGENIEVICH , OKUN ILYA MATUSOVICH , SAVCHUK NIKOLAY FILIPPOVICH , KRAVCHENKO DMITRI VLADIMIROVIC , RIZHOVA ELENA ALEXANDROVNA , ALYABIEV SERGEY BORISOVICH , KHVAT ALEXANDER VIKTOROVICH
发明人： IVASHCHENKO ANDREY ALEXANDROVICH , IVASHCHENKO ALEXANDER VASILIEVICH , TKACHENKO SERGEY YEVGENIEVICH , OKUN ILYA MATUSOVICH , SAVCHUK NIKOLAY FILIPPOVICH , KRAVCHENKO DMITRI VLADIMIROVICH , RIZHOVA ELENA ALEXANDROVNA , ALYABIEV SERGEY BORISOVICH , KHVAT ALEXANDER VIKTOROVICH
IPC分类号： C07D491/048 , C07D487/04 , C07D491/113 , C07D491/147 , C07D495/04 , C07D495/14 , C07D498/04 , C07D498/14 , C07D513/04
CPC分类号： C07D487/04 , C07D491/048 , C07D491/113 , C07D491/147 , C07D495/04 , C07D495/14 , C07D498/04 , C07D498/14 , C07D513/04
摘要： The invention relates to novel annelated azaheterocycles of general formula 1, containing a pyrimidine fragment in the form of free bases or pharmaceutically acceptable salts, to pharmaceutical compositions containing said compounds and to the use of said compounds for producing medicinal preparations and therapeutic cocktails for treating human and homothermal diseases caused by a class I phosphoinositol kinase (PI3Ks) activity (and mutant isoforms thereof), in particular oncological diseases, to the use of said compounds as "molecular pharmacological instruments" for studying (in vitro and in vivo) biochemical mechanisms of (PI3Ks) kinase action, in particular class I kinases (PI3Ks) and mutant isoforms thereof. In the formula 1, X is an oxygen atom,a sulphur atom or an optionally nitrogen-substituted group; Y is a nitrogen atom or an optionally carbon-substituted CH group; Z is an oxygen atom; R1 is a hydrogen atom or optionally substituted C1-C6 alkyl or Z is a nitrogen atom which, together with an carbon atom, to which it is bound, form, via Z and R1, an optionally substituted imidazoline cycle; R2 and R3, independently from each other, are optionally substituted alkyl, optionally substituted aryl or heterocycle, wherein Y is an optionally carbon-substituted CH group, X=O,S, or R2 is hydrogen, R3 is substituted aminoalkyl or optionally substituted azaheterocyclyl alkyl, wherein optionally substituted azaheterocyclyl alkyl or R2 is hydrogen, R3 is substituted aminoalkyl or optionally substituted azaheterocyclyl alkyl, R1 is substituted aminoalkyl, substituted hydroxy alkyl or optionally substituted azaheterocyclyl alkyl, Y is an optionally carbon-substituted CH group, X=O,S; R4 is hydrogen or lower alkyl.
摘要翻译：本发明涉及包含游离碱或药学上可接受的盐形式的嘧啶片段的通式1的新型环状氮杂杂环化合物，其含有所述化合物的药物组合物和所述化合物用于制备用于治疗人的药物制剂和治疗性鸡尾酒的用途由I类磷酸肌醇激酶（PI3Ks）活性引起的等温疾病（及其突变体同种型）特别是肿瘤疾病使用所述化合物作为“分子药理学仪器”用于研究（体外和体内）生物化学机制（PI3Ks）激酶作用，特别是I类激酶（PI3Ks）及其突变体同种型。在式1中，X是氧原子，硫原子或任选的氮取代基; Y是氮原子或任选被碳取代的CH基团; Z是氧原子; R 1是氢原子或任选取代的C 1 -C 6烷基或Z是氮原子，与氮原子一起通过Z和R 1与其结合的碳原子一起形成任选取代的咪唑啉循环; R 2和R 3彼此独立地是任选取代的烷基，任选取代的芳基或杂环，其中Y是任选被碳取代的CH基团，X = O，S或R 2是氢，R 3是取代的氨基烷基或任选取代的杂环基烷基，其中任选取代的杂氮杂环烷基或R 2是氢，R 3是取代的氨基烷基或任选取代的杂环基烷基，R 1是取代的氨基烷基，取代的羟基烷基或任选取代的杂氮杂环烷基，Y是任选被碳取代的CH基团，X = S; R4是氢或低级烷基。

2. 发明申请

WO2007105989A3 1-OXO-3-(1H-INDOLE)-3-IL-1,2,3,4-TETRAHYDROISOXYNOLINES, METHODS FOR THE PRODUCTION THEREOF, COMBINATORIC LIBRARY AND FOCUSED LIBRARY 审中-公开
标题翻译： 1-OXO-3-（1H-吲哚）-3-IL-1,2,3,4-四氢异喹啉，其制备方法，联合文库和重点文库
公开(公告)号：WO2007105989A3
公开(公告)日：2007-11-22
申请号：PCT/RU2007000116
申请日：2007-03-12
申请人： IVASHCHENKO ANDREY ALEXANDROVI , ALLA CHEM LLC , IVASHCHENKO ALEXANDER VASILIEV , KRAVCHENKO DMITRI VLADIMIROVIC , LOSEVA MARINA VASILIEVNA , OKUN ILYA MATUSOVICH , TKACHENKO SERGEY YEVGENIEVICH , KHVAT ALEXANDER VIKTOROVICH
发明人： IVASHCHENKO ALEXANDER VASILIEV , KRAVCHENKO DMITRI VLADIMIROVIC , LOSEVA MARINA VASILIEVNA , OKUN ILYA MATUSOVICH , TKACHENKO SERGEY YEVGENIEVICH , KHVAT ALEXANDER VIKTOROVICH
IPC分类号： C07D401/04 , A61P35/00 , C07D209/00 , C07D217/00 , C07D277/00 , C07D295/00 , C07D307/00 , C07D317/48 , C07D333/00 , C07D401/14 , C07D405/14 , C07D409/14 , C07D413/14 , C07D417/14 , C07D491/113 , C40B40/04
CPC分类号： C07D401/04 , C07D401/14 , C07D405/14 , C07D417/14 , C07D491/10
摘要： The invention relates to novel 1-oxo-3-(1h-indole)-3-il-1,2,3,4-tetrahydroisoxynolines and to the cis- and trans-isomers thereof exhibiting protein kinase inhibiting properties, to methods for the production thereof and to combinatoric and focused libraries for separating leader compounds. 1-oxo-3-(1h-indole)-3-il-1,2,3,4-tetrahydroisoxynolines correspond to general formulas 1 and 2, wherein R 1 , R 2 and R 4 , independently from each other are, a cyclic system substituent selected from hydrogen and alkyl, R 3 is an aminogroup substituent selected from alkyl, cycloalkyl or alkyl, possibly substituted with an aryl, heteroaryl, heterocyclyl, alkoxy, amine, alkylamine and dialkylamine group, R 5 and R 6 are, independently from each other, an amino group substituent selected from hydrogen, aryl, heteroaryl, heterocyclyl, cycloalkyl, cycloalkenyl, alkyl or alkyl, possibly substituted with aryl, heteroaryl, heterocyclyl, cycloalkyl, cycloalkenyl, alkoxy, amino, alkylamine, dialkylamine, aryl alkylamine, or R 5 and R 6 forms, together with a nitrogen atom with which they are bound, a possibly substituted azaheterocycle. A method for obtaining compounds of general formula 1 consists in interacting corresponding indole-3-ilmethylenamines and homophtalic anhydrides in an organic solvent medium. A method for obtaining compounds of general formula 2 consists in treating the compounds of formula 1 with thionyl chloride or with 1,1'-carbonyldiimidazole in such a way that the respective derivatives are obtain and interact with respective amines of general formula 6 in the organic solvent medium.
摘要翻译：本发明涉及显示蛋白激酶抑制性能的新的1-氧-3-（1h-吲哚）-3-I-1，2，3，4-tetrahydroisoxynolines及其顺式和反式异构体，涉及其生产以及用于分离前导化合物的组合文库和聚焦文库。 1-氧代-3-（1H-吲哚）-3-I-1,2,3,4-四氢异恶唑啉对应于通式1和2，其中R 1，R 2，其中R 1和R 4彼此独立地是选自氢和烷基的环状系统取代基，R 3是选自烷基，环烷基或烷基的氨基基团取代基，可能被芳基，杂芳基，杂环基，烷氧基，胺，烷基胺和二烷基胺基团取代，R 5和R 6相互独立地为氨基取代基其选自氢，芳基，杂芳基，杂环基，环烷基，环烯基，可能被芳基，杂芳基，杂环基，环烷基，环烯基，烷氧基，氨基，烷基胺，二烷基胺，芳基烷基胺或R 5取代的烷基或烷基。 R 6和R 6与它们所结合的氮原子一起形成可能被取代的氮杂杂环。获得通式1的化合物的方法在于在有机溶剂介质中相互作用相应的吲哚-3-甲硅烷胺和均聚酸酐。获得通式2的化合物的方法在于用亚硫酰氯或用1,1'-羰基二咪唑处理式1的化合物，使得相应的衍生物在有机相中得到并与相应的通式6的胺相互作用溶剂介质。

3. 发明申请

WO2005105805A9 ANNELATED CARBAMOYLASE-HETEROCYCLES, FOCUSED LIBRARY, PHARMACEUTICAL COMPOSITIONS AND METHODS FOR THE PRODUCTION THEREOF 审中-公开
标题翻译：苯胺羧酸酯 - 杂环化合物，聚焦图谱，药物组合物及其生产方法
公开(公告)号：WO2005105805A9
公开(公告)日：2006-01-19
申请号：PCT/RU2005000235
申请日：2005-04-29
申请人： CHEMICAL DIVERSITY RES INST LT , IVASHCHENKO ALEXANDER VASILIEV , VVEDENSKY VLADIMIR YURIEVICH , ILYN ALEKSEI PETROVICH , KYSEL VOLODYMYR MIKHAILOVICH , KHVAT ALEXANDER VIKTOROVICH , KUZOVKOVA YULIA ALEKSANDROVNA , KUTEPOV SERGEY ALEKSANDROVICH , DMITRIEVA IRINA GENNADIEVNA , ZOLOTAREV DENIS ANATOLIEVICH , TKACHENKO SERGEY YEVGENIEVICH , OKUN ILYA MATUSOVICH , KRAVCHENKO DMITRI VLADIMIROVIC , KOBAK VLADIMIR VASILIEVICH , TRIFILENKOV ANDREI SERGEEVICH , MISHUNINA YULIA SERAFIMOVA , LOSEVA MARINA VASILIEVNA , RIZHOVA ELENA ALEXANDROVNA , PARCHINSKY VLADISLAV ZENONOVIC , TSIRULNIKOV SERGEY ALEXANDROVI , KYSELEV ALEXANDR SERGEEVICH
发明人： IVASHCHENKO ALEXANDER VASILIEV , VVEDENSKY VLADIMIR YURIEVICH , ILYN ALEKSEI PETROVICH , KYSEL VOLODYMYR MIKHAILOVICH , KHVAT ALEXANDER VIKTOROVICH , KUZOVKOVA YULIA ALEKSANDROVNA , KUTEPOV SERGEY ALEKSANDROVICH , DMITRIEVA IRINA GENNADIEVNA , ZOLOTAREV DENIS ANATOLIEVICH , TKACHENKO SERGEY YEVGENIEVICH , OKUN ILYA MATUSOVICH , KRAVCHENKO DMITRI VLADIMIROVIC , KOBAK VLADIMIR VASILIEVICH , TRIFILENKOV ANDREI SERGEEVICH , MISHUNINA YULIA SERAFIMOVA , LOSEVA MARINA VASILIEVNA , RIZHOVA ELENA ALEXANDROVNA , PARCHINSKY VLADISLAV ZENONOVIC , TSIRULNIKOV SERGEY ALEXANDROVI , KYSELEV ALEXANDR SERGEEVICH
IPC分类号： A61K31/4985 , A61K31/55 , A61K31/5513 , A61K31/5517 , A61K31/554 , A61P35/00 , C07D471/04 , C07D487/04 , C07D487/14 , C07D493/14 , C07D495/14 , C07D498/04 , C07D498/14 , C07D513/04 , C07D513/14 , C40B40/04
CPC分类号： C40B40/04 , A61K31/4985 , A61K31/5513 , A61K31/5517 , A61K31/554 , C07D471/04 , C07D487/04 , C07D487/14 , C07D493/14 , C07D495/14 , C07D513/04
摘要： The invention relates to novel carbamoylase-heterocycles which are of interest in the form of potential physiologically active agents (receptor agonists, antagonists and modulators, ferment inhibitors, oncolytics, antibacterial and antiparasitic agents, etc), to a focused library comprising carbamoylase-heterocycles, a pharmaceutical composition containing said carbamoylase-heterocycles in the form of an active substance and to methods for the production and the use thereof. The inventive carbamoylase-heterocycles are of general formula 1, wherein W is 6-oxopiperazine,[1,4]diazepan, [1,4] tiazepan or [1,4] oxazepan cycle annelated with at least one optionally substituted or optionally condensed heterocycle Q;
摘要翻译：本发明涉及以潜在的生理活性剂（受体激动剂，拮抗剂和调节剂，发酵抑制剂，溶瘤剂，抗菌剂和抗寄生虫剂等）的形式感兴趣的新的氨甲酰化酶 - 杂环，包括氨基甲酰基 - 杂环，含有活性物质形式的所述氨基甲酰基 - 杂环的药物组合物及其制备方法和用途。本发明的氨基甲酰化酶 - 杂环具有通式1，其中W是6-氧代哌嗪，[1,4]二氮杂环庚烷，[1,4]噻唑烷或[1,4]氧氮杂环与至少一个任选取代或任选稠合的杂环 Q; <子/

4. 发明申请

WO2007136300A2 SUBSTITUTED INDOLES AND A METHOD FOR THE PRODUCTION AND USE THEREOF 审中-公开
标题翻译：取代的吲哚及其生产和使用方法
公开(公告)号：WO2007136300A2
公开(公告)日：2007-11-29
申请号：PCT/RU2007000244
申请日：2007-05-17
申请人： ALLA CHEM LLC , IVASCHENKO ANDREY ALEXANDROVIC , TKACHENKO SERGEY YEVGENIEVICH , KHVAT ALEXANDER VIKTOROVICH , MITKIN OLEG DMITRIEVICH , OKUN ILYA MATUSOVICH , KYSELVEV ALEXANDR SERGEEVICH , KYSIL VOLODYMYR MIKHAILOVICH , SAVCHUK NIKOLAY FILIPPOVICH , IVASHCHENKO ALEXANDER VASILIEV
发明人： IVASCHENKO ANDREY ALEXANDROVIC , TKACHENKO SERGEY YEVGENIEVICH , KHVAT ALEXANDER VIKTOROVICH , MITKIN OLEG DMITRIEVICH , OKUN ILYA MATUSOVICH , KYSELVEV ALEXANDR SERGEEVICH , KYSIL VOLODYMYR MIKHAILOVICH , SAVCHUK NIKOLAY FILIPPOVICH , IVASHCHENKO ALEXANDER VASILIEV
IPC分类号： C07D209/42 , A61K31/405 , A61K31/407 , A61K31/416 , A61K31/4465 , A61K31/454 , A61K31/4709 , A61K31/506 , A61K31/5365 , A61K31/55 , A61P31/12 , A61P31/16 , C07D401/04 , C07D401/06 , C07D401/14 , C07D403/04 , C07D403/06 , C07D405/04 , C07D409/04 , C07D413/14 , C07D498/04
CPC分类号： C07D401/14 , C07D209/42 , C07D401/04 , C07D401/06 , C07D403/04 , C07D403/06 , C07D405/04 , C07D409/04 , C07D413/14 , C07D498/04
摘要： The invention relates to novel substituted indoles, to the use thereof in the form of pharmacological composition substances and to use of said composition for producing medicinal preparations used for preventing and treating viral diseases, in particular caused by viruses of infectious hepatitis (HCV, HBV), human immune deficiency (HIV), atypical pneumonia (SARS) and bird flu. The invention proposes novel substituted indoles of general formula (1) or the racemates or the optical isomers or the pharmaceutically acceptable salts and/or hydrates thereof, wherein R 1 , R 1 4
摘要翻译：本发明涉及以药物组合物物质形式使用的新型取代的吲哚，以及所述组合物用于制备用于预防和治疗病毒性疾病，特别是由感染性肝炎（HCV，HBV）病毒引起的病毒性疾病的药物制剂的用途，，人类免疫缺陷（HIV），非典型肺炎（SARS）和禽流感。本发明提出了通式（1）的新型取代吲哚或其外消旋物或光学异构体或其药学上可接受的盐和/或水合物，其中R 1，R 1， ⁴

5. 发明申请

WO2005018531A3 PHARMACEUTICAL COMPOSITIONS, AZO-HETEROCYCLIC COMPOUNDS AND METHOD FOR THE PRODUCTION AND USE THEREOF 审中-公开
标题翻译：药物组合物，偶氮杂环化合物及其生产和使用方法
公开(公告)号：WO2005018531A3
公开(公告)日：2005-05-12
申请号：PCT/RU2004000331
申请日：2004-08-25
申请人： CHEMICAL DIVERSITY RES INST LT , IVASHCHENKO ALEXANDER VASILIEV , ILYIN ALEXEY PETROVICH , KOBAK VLADIMIR VASILIEVICH , KRAVCHENKO DMITRI VLADIMIROVIC , KHVAT ALEXANDER VIKTOROVICH , TKACHENKO SERGEY YEVGENIEVICH , OKUN ILYA MATUSOVICH
发明人： IVASHCHENKO ALEXANDER VASILIEV , ILYIN ALEXEY PETROVICH , KOBAK VLADIMIR VASILIEVICH , KRAVCHENKO DMITRI VLADIMIROVIC , KHVAT ALEXANDER VIKTOROVICH , TKACHENKO SERGEY YEVGENIEVICH , OKUN ILYA MATUSOVICH
IPC分类号： A61K20060101 , A61K31/404 , A61K31/427 , A61K31/498 , A61K31/519 , A61K31/52 , A61K31/525 , A61K31/5377 , A61P9/10 , A61P25/00 , A61P25/18 , A61P25/28 , A61P31/12 , A61P31/18 , C07D209/34 , C07D241/44 , C07D401/06 , C07D401/12 , C07D401/14 , C07D403/06 , C07D405/14 , C07D409/12 , C07D413/12 , C07D417/12 , C07D417/14 , C07D475/14 , C07D487/04 , C07D491/12 , C07D513/04 , C07D513/08 , C07D513/14
CPC分类号： A61K31/404 , A61K31/427 , A61K31/498 , A61K31/519 , A61K31/52 , A61K31/525 , A61K31/5377 , C07D241/44 , C07D417/04 , C07D417/14 , C07D475/14
摘要： The inventive pharmaceutical composition exhibits an inhibiting activity with respect to serine proteinase (Kaspaz) and comprises an active substance embodied in the form of a pharmaceutically acceptable quantity of an azo-heterocyclic compound of general formula 1, 2 and 3 or the salts thereof with pharmacologically acceptable acid, hydrate one N-oxide.
摘要翻译：本发明的药物组合物对丝氨酸蛋白酶（Kaspaz）表现出抑制活性，并且包含以可药用量的通式1,2和3的偶氮杂环化合物或其盐的药理学上可接受的量可接受的酸，水合一种N-氧化物。

6. 发明申请

WO2009077956A3 HETEROCYCLIC INHIBITORS OF AN Hh-SIGNAL CASCADE, MEDICINAL COMPOSITIONS BASED THEREON AND METHODS FOR TREATING DISEASES CAUSED BY THE ABERRANT ACTIVITY OF AN Hh-SIGNAL SYSTEM 审中-公开
标题翻译： Hh信号级联的杂环抑制剂，基于其的药物组合物以及治疗由Hh信号系统的异常活性引起的疾病的方法
公开(公告)号：WO2009077956A3
公开(公告)日：2009-10-22
申请号：PCT/IB2008055258
申请日：2008-12-12
申请人： IVASHCHENKO ANDREY ALEXANDROVICH , ALLA CHEM LLC , LAVROVSKY YAN VADIMOVICH , LAKNER FRED , MALYARCHUK SERGEY VIKTOROVICH , OKUN ILYA MATUSOVICH , SAVCHUK NIKOLAY FILIPPOVICH , TKACHENKO SERGEY YEVGENIEVICH , KHVAT ALEXANDER VIKTOROVICH , IVASHCHENKO ALEXANDER VASILIEVICH
发明人： IVASHCHENKO ANDREY ALEXANDROVICH , LAVROVSKY YAN VADIMOVICH , LAKNER FRED , MALYARCHUK SERGEY VIKTOROVICH , OKUN ILYA MATUSOVICH , SAVCHUK NIKOLAY FILIPPOVICH , TKACHENKO SERGEY YEVGENIEVICH , KHVAT ALEXANDER VIKTOROVICH , IVASHCHENKO ALEXANDER VASILIEVICH
IPC分类号： C07D487/04 , A61K31/407 , A61K31/437 , A61K31/4375 , A61K31/4535 , A61K31/4545 , A61K31/519 , A61K31/542 , A61P35/00 , C07D215/58 , C07D401/04 , C07D495/04 , C07D498/04 , C07D513/04
CPC分类号： C07D487/04 , A61K9/0019 , A61K9/2018 , A61K9/205 , A61K9/2059 , A61K9/4858 , C07D215/58 , C07D401/04 , C07D471/04 , C07D495/04 , C07D513/04
摘要： The invention relates to novel heterocyclic compounds and to the use thereof, to pharmaceutical compositions containing said chemical compounds as an active ingredient and to the use thereof for producing medicinal preparations for the human being and warm-blood animals for treating diseases caused by the aberrant activity of an Hedgehog (Hh)-signal system, in particular oncological diseases. The invention also relates to the use of the above-mentioned compounds in the form of 'molecular pharmacological tools' for examining (in vitro and in vivo) the biochemical features of the Hh-signal system, in particular, the interaction of Hh protein and transmembrane proteins, namely, suppressor Patched (Ptc) and protooncogenic proteins. The eight groups of the claimed compounds comprise the derivatives of 2,6-dihydro-7H-pyrazolo[3,4-d] pyridazine-7-one and 1,4-dihydropyrazolo[3,4-b][1,4]thiazine-5-one; N-acidylated 4-imidazo[1,2-a] pyrimidine-2-il-anilines; ([4H-thino[3,2-b]pyrrol-5-il) carbonyl]piperidine-4-carbonic acid amides; 2-(4carbomoilpyperidine-1-il)-isonicotinic acid amides; N-sylphonyl-1,2,3,4-tetrahydroquinoline-6-carbonic acid amides; and pyridine 2-amino-4,5,6,7-tetrahydrothieno[2,3-c] N-acidylated 3-azole derivatives.
摘要翻译：本发明涉及新的杂环化合物及其用途，含有所述化合物作为活性成分的药物组合物及其用于制备用于治疗人类和温血动物以治疗由异常活性引起的疾病的药物制剂的用途刺猬（Hh） - 信号系统，特别是肿瘤疾病。本发明还涉及“分子药理学工具”形式的上述化合物用于检查（体外和体内）Hh信号系统的生化特征，特别是Hh蛋白与跨膜蛋白，即抑制剂Patched（Ptc）和原癌基因蛋白。八组要求保护的化合物包括2,6-二氢-7H-吡唑并[3,4-d]哒嗪-7-酮和1,4-二氢吡唑并[3,4-b] [1,4] 噻嗪-5-酮; N-酸化的4-咪唑并[1,2-a]嘧啶-2-基 - 苯胺; （[4H-噻吩并[3,2-b]吡咯-5-基）羰基]哌啶-4-碳酸酰胺; 2-（4-氨基甲酰基哌啶-1-基） - 异烟酸酰胺; N-磺酰基-1,2,3,4-四氢喹啉-6-碳酸酰胺; 和吡啶2-氨基-4,5,6,7-四氢噻吩并[2,3-c] N-酸化的3-唑衍生物。

7. 发明申请

WO2014133414A3 HETEROCYCLIC TGR5 BILE ACID RECEPTOR AGONISTS, PHARMACEUTICAL COMPOSITION, METHODS FOR THE PRODUCTION AND USE THEREOF 审中-公开
标题翻译：杂环TGR5胆酸受体激动剂，药物组合物，其生产和使用方法
公开(公告)号：WO2014133414A3
公开(公告)日：2014-12-18
申请号：PCT/RU2014000108
申请日：2014-02-19
申请人： IVASCHENKO ANDREY ALEXANDROVICH , ALLA CHEM LLC , SAVCHUK NIKOLAY FILIPPOVICH
发明人： IVASCHENKO ANDREY ALEXANDROVICH , SAVCHUK NIKOLAY FILIPPOVICH , TKACHENKO SERGEY YEVGENIEVICH , KHVAT ALEXANDER VIKTOROVICH
IPC分类号： C07D267/14 , A61K31/553 , A61P3/06 , A61P3/08 , A61P3/10 , C07D413/12 , C07D413/14
CPC分类号： C07D267/12 , C07D413/06 , C07D413/12 , C07D417/12
摘要： 1. Compounds of general formula I, or racemic mixtures thereof, or individual optical isomers thereof, or pharmaceutically acceptable salts and/or hydrates thereof, wherein: X is the amino group R'R''N, optionally substituted or unsubstituted with identical substituents R' and R'', or a substituted oxy group; the R'R''N group is a non-aromatic azaheterocycle, preferably azetidine, pyrrolidine, piperidine, morpholine, thiomorpholine, piperazine, homopiperidine or homopiperazine; the amino group substituents R' and R'' are hydrogen, alkyl, substituted alkyl, cycloalkyl, aryl, heteroaryl, heterocyclyl, alkenyl, cycloalkenyl, alkynyl, acyl, aroyl, heteroaroyl, alkylsulphonyl, arylsulphonyl, heteroarylsulphonyl, alkoxycarbonyl, aryloxycarbonyl, araloxycarbonyl, alkylaminocarbonyl, arylaminocarbonyl, heteroarylaminocarbonyl, heterocyclylaminocarbonyl, alkylaminothiocarbonyl, arylaminothiocarbonyl, heteroarylaminothiocarbonyl, heterocyclylaminothiocarbonyl, optionally substituted aminosulphonyl, the R'R''N group may be a non-aromatic azaheterocycle, preferably azetidine, pyrrolidine, piperidine, morpholine, thiomorpholine, piperazine, homopiperidine or homopiperazine; and the substituted oxy group is a hydroxy group in which hydrogen is substituted with alkyl, alkenyl, cycloalkyl, cycloalkenyl, aryl, hetaryl and heterocyclyl, or acyl, or an aminocarbonyl group or an oxycarboyl group; R1a and R1b are hydrogen and alkyl, or R1a and R1b together form a -(CH2)n- polymethylene chain, wherein n=2-5; R1c and R1d are hydrogen and alkyl, or R1c and R1d together form a -(CH2)n- polymethylene chain, wherein n=2-5; R2 is an acyl group, a thioacyl group, a substituted oxycarbonyl group, a substituted amidine group, a substituted aminocarbonyl group, a substituted aminothiocarbonyl group or a sulphonyl group; R3 is hydrogen, C1-C6 alkyl, an alkoxy group, halogen, CF3, CN.
摘要翻译： 1.通式I化合物或其外消旋混合物或其各自的光学异构体或其药学上可接受的盐和/或水合物，其中：X为任选取代或未取代的具有相同取代基的氨基R'R''N R'和R“，或取代的氧基; R'R'N基是非芳族氮杂环，优选氮杂环丁烷，吡咯烷，哌啶，吗啉，硫代吗啉，哌嗪，高哌啶或高哌嗪; 酰基，芳酰基，杂芳酰基，烷基磺酰基，芳基磺酰基，杂芳基磺酰基，烷氧基羰基，芳氧基羰基，芳氧基羰基，芳氧基羰基，芳氧基羰基，烷基氨基羰基，芳基氨基羰基，杂芳基氨基羰基，杂环基氨基羰基，杂芳基氨基硫代羰基，杂芳基氨基硫代羰基，杂芳基氨基硫代羰基，杂环基氨基硫代羰基，任选取代的氨基磺酰基，R'R''N基团可以是非芳族氮杂环，优选氮杂环丁烷，吡咯烷，哌啶，吗啉，硫代吗啉，哌嗪，高哌啶或高哌嗪; 取代的氧基是其中氢被烷基，烯基，环烷基，环烯基，芳基，杂芳基和杂环基或酰基或氨基羰基或氧代羰基取代的羟基; R1a和R1b是氢和烷基，或R1a和R1b一起形成 - （CH2）n-多亚甲基链，其中n = 2-5; R1c和R1d是氢和烷基，或R1c和R1d一起形成 - （CH2）n-多亚甲基链，其中n = 2-5; R2是酰基，硫代酰基，取代的氧羰基，取代的脒基，取代的氨基羰基，取代的氨基硫代羰基或磺酰基; R3是氢，C1-C6烷基，烷氧基，卤素，CF3，CN。

10. 发明专利

CO2019014516A2 Una nanosuspensión farmacéutica para el tratamiento de la infección por vih 未知
公开(公告)号：CO2019014516A2
公开(公告)日：2020-01-17
申请号：CO2019014516
申请日：2019-12-20
申请人： IVACHTCHENKO ALEXANDRE VASILIEVICH , IVASHCHENKO ANDREY ALEXANDROVICH , SAVCHUK NIKOLAY FILIPPOVICH , IVACHTCHENKO ALENA ALEXANDROVNA , ALLA CHEM LLC
发明人： IVASHCHENKO ANDREY ALEXANDROVICH , SAVCHUK NIKOLAY FILIPPOVICH , KHVAT ALEXANDER VIKTOROVICH
IPC分类号： A61K31/18 , A61K9/10 , A61K9/19 , A61P31/18 , B82Y5/00 , B82Y40/00
摘要： La presente invención se refiere a una composición farmacéutica (nanosuspensión) para un fármaco inyectable de acción prolongada (LAI) para la terapia de apoyo a largo plazo del VIH/SIDA. Una nanosuspensión farmacéutica para ser utilizada como un fármaco inyectable para la terapia de apoyo a largo plazo de la infección por VIH que comprende una composición que contiene, como ingrediente activo, un compuesto de fórmula general 1 en forma cristalina o policristalina , en donde es C2H5CON-Na+, NH2.

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