利索-全球专利检索

  1. 登录
  2. 注册

搜索结果

51 条记录 (耗时 0.026 秒)

    (EN) 3-sulfonyl-pyrazolo[1,5-a] pyrimidines / antagonists of serotonin 5-HT6 receptors, methods for the production and the use thereof
    21.
    发明授权
    (EN) 3-sulfonyl-pyrazolo[1,5-a] pyrimidines / antagonists of serotonin 5-HT6 receptors, methods for the production and the use thereof 有权
    （EN）3-磺酰基 - 吡唑并[1,5-a]嘧啶/ 5-羟色胺5-HT 6受体的拮抗剂，生产方法及其用途

    公开(公告)号：US08552005B2

    公开(公告)日：2013-10-08

    申请号：US12812728

    申请日：2009-01-23

    申请人： Andrey Alexandrovich Ivashchenko ,  Alexander Vasilievich Ivashchenko ,  Nikolay Filippovich Savchuk

    发明人： Andrey Alexandrovich Ivashchenko ,  Alexander Vasilievich Ivashchenko ,  Nikolay Filippovich Savchuk

    IPC分类号： A01N43/90 ,  A01N43/00 ,  A61K31/519 ,  A61K31/33 ,  C07D487/00

    CPC分类号： C07D487/04

    摘要： The present invention relates to novel substituted 3-(arylsulfonyl)pyrazolo[1,5-a]pyrimidines of general formula 1 pharmaceutically acceptable salts and/or hydrates, to novel serotonin 5-HT6 receptor antagonists, to novel drug substances, pharmaceutical compositions, medicaments and methods for their preparation and use for treatment and prophylaxis of pathological states and diseases of CNS, pathogenesis of which is associated with disturbance of serotonin 5-HT6 receptor activation.In compounds of general formula 1 Ar represents optionally substituted aryl or heterocyclyl; R1, R2 and R3 independently of each other represent hydrogen, C1-C3 alkyl or phenyl; R4 represents hydrogen, optionally substituted C1-C5 alkyl, substituted hydroxyl group or substituted sulfanyl group.

    摘要翻译： 本发明涉及通式1的药学上可接受的盐和/或水合物的新的取代的3-（芳基磺酰基）吡唑并[1,5-a]嘧啶新颖的5-羟色胺5-HT 6受体拮抗剂，新药物，药物组合物， 药物及其制备方法，用于治疗和预防CNS的病理状态和疾病，其发病机制与血清素5-HT6受体激活的干扰有关。 在通式1的化合物中Ar表示任选取代的芳基或杂环基; R 1，R 2和R 3彼此独立地表示氢，C 1 -C 3烷基或苯基; R 4表示氢，任选取代的C 1 -C 5烷基，取代的羟基或取代的硫烷基。

    (EN) substituted 2-amino-3-sulfonyl-pyrazolo[1,5-A] pyrimidines/antagonists of serotonin 5-HT6 receptors, methods for the production and the use thereof
    22.
    发明授权
    (EN) substituted 2-amino-3-sulfonyl-pyrazolo[1,5-A] pyrimidines/antagonists of serotonin 5-HT6 receptors, methods for the production and the use thereof 有权
    （EN）取代的2-氨基-3-磺酰基 - 吡唑并[1,5-A]嘧啶/ 5-羟色胺5-HT 6受体的拮抗剂，其制备方法及用途

    公开(公告)号：US08309559B2

    公开(公告)日：2012-11-13

    申请号：US12812733

    申请日：2009-01-23

    申请人： Nikolay Filippovich Savchuk ,  Alexander Vasilievich Ivashchenko

    发明人： Nikolay Filippovich Savchuk ,  Alexander Vasilievich Ivashchenko

    IPC分类号： A01N43/90 ,  A61K31/519 ,  C07D487/00

    CPC分类号： C07D487/04

    摘要： The present invention relates to novel substituted 2-amino-3-(arylsulfonyl)pyrazolo[1,5-a]pyrimidines of general formula 1, to serotonin 5-HT6 receptor antagonists, to novel drug substances and pharmaceutical compositions, to medicaments, methods for preparation thereof, and to methods for prophylaxis and treatment of various CNS diseases, pathogenesis of which is associated with disturbance of monoaminergic signaling pathways, more specifically over- or hypo-activation of serotonin 5-HT6 receptors. Ar represents optionally substituted aryl or optionally substituted heterocyclyl; R1 and R3 independently of each other represent C1-C3 alkyl or aryl; R2 represents hydrogen or C1-C3 alkyl; R41, and R42 independently of each other represent hydrogen, optionally substituted C1-C3 alkyl or optionally substituted phenyl, or R41, and R42 together with nitrogen atom they are attached to form optionally substituted heterocyclyl.

    摘要翻译： 本发明涉及通式1的新的取代的2-氨基-3-（芳基磺酰基）吡唑并[1,5-a]嘧啶，5-羟色胺5-HT 6受体拮抗剂，新药物和药物组合物，药物，方法 以及用于预防和治疗各种CNS疾病的方法，其发病机制与单胺能信号通路的紊乱相关，更具体地说是5-羟色胺5-HT 6受体的过激活或低激活。 Ar表示任选取代的芳基或任选取代的杂环基; R1和R3彼此独立地表示C1-C3烷基或芳基; R2代表氢或C1-C3烷基; R 41和R 42彼此独立地表示氢，任选取代的C 1 -C 3烷基或任选取代的苯基，或R 41和R 42与它们连接的氮原子一起形成任选取代的杂环基。

    Macroheterocyclic nucleoside derivatives and their analogues, production and use thereof
    27.
    发明授权
    Macroheterocyclic nucleoside derivatives and their analogues, production and use thereof 有权

    公开(公告)号：US10266558B2

    公开(公告)日：2019-04-23

    申请号：US15287805

    申请日：2016-10-07

    申请人： Alexandre Vasilievich Ivachtchenko ,  Andrey Alexandrovich Ivashchenko ,  Nikolay Filippovich Savchuk ,  ASAVI, LLC ,  Alena Alexandrovna Ivachtchenko ,  Oleg Dmitrievich Mitkin

    发明人： Alexandre Vasilievich Ivachtchenko ,  Oleg Dmitrievich Mitkin ,  Andrey Alexandrovich Ivashchenko ,  Alena Alexandrovna Ivachtchenko ,  Nikolay Filippovich Savchuk

    IPC分类号： A61K31/70 ,  A01N43/04 ,  C07H19/10 ,  A61K31/7072 ,  A61K45/06 ,  A61K31/7068 ,  A61K31/7076 ,  A61K31/708 ,  A61K31/7064 ,  A61K31/7056 ,  A61K31/706 ,  A61K31/7084 ,  A61K31/7052

    摘要： Nucleosides and nucleotides (nucleos(t)ides) have been in clinical use for almost 50 years and have become cornerstones of treatment for patients with viral infections or cancer. The approval of several additional drugs over the past decade demonstrates that this family still possesses strong potential. Therefore nucleos(t)ide are of great interest as promising chemotherapeutic agents, including: 2′-deoxy-L-uridine (CAS 31501-19-6), 2′-deoxy-D-uridine (CAS 951-78-0), telbivudine (CAS 3424-98-4), zidovudine (AZT, CAS 30516-87-1), trifluridine (CAS 70-00-8), clevudine (CAS 163252-36-6), PSI-6206 (CAS 863329-66-2), 2′-(S)-2′-chloro-2′-deoxy-2′-fluorouridine (CAS 1673560-41-2), ND06954 (CAS 114248-23-6), stavudine (CAS 3056-17-5), 5-ethynyltavudine (Festinavir, CAS 634907-30-5), torcitabine (CAS 40093-94-5), (−)-beta-D-(2R,4R)-dioxolane-thymine (DOT, 1-((2R,4R)-2-(hydroxymethyl)-1,3-dioxolan-4-yl)-5-methyl-2,4(1H,3H)-pyrimidinedione, CAS No. 127658-07-5), 2-(6-amino-purin-9-yl)-ethanol (CAS 707-99-3), 2′-C-methylcytidine (CAS 20724-73-6), PSI-6130 (CAS 817204-33-4), gemcitabine (CAS 95058-81-4), 2′-chloro-2′-deoxy-2′-fluorocytidine (CAS 1786426-19-4), 2′,2′-dichloro-2′-deoxycytidine (CAS 1703785-65-2), 2′-C-methylcytidine (CAS 20724-73-6), PSI-6130 (CAS 817204-33-4), lamivudine (3TC, CAS 134678-17-4), emtricitabine (CAS 143491-57-0), 2′-deoxyadenosine (CAS 958-09-8), 2′-deoxy-β-L-adenosine (CAS 14365-45-8), 2′-deoxy-4′-C-ethynyl-2-fluoroadenosine (CAS 865363-93-5), didanosine (CAS 69655-05-6), entecavir (CAS 209216-23-9), FMCA (CAS 1307273-70-6), dioxolane-G (DOG, CAS 145514-01-8), β-D-2′-deoxy-2′-(R)-fluoro-2′-β-C-methylguanosine (CAS No 817204-45-8), abacavir (ABC, CAS 136470-78-5), dioxolane-A (DOA, CAS #145514-02-9), [(2R,4R)-4-(6-cyclopropylamino-purin-9-yl)-[1,3]dioxolan-2-yl]-methanol (CAS 1446751-04-7), amdoxovir (AMDX, CAS 145514-04-1), (R)-1-(6-amino-purin-9-yl)-propan-2-ol (CAS 14047-28-0), and [(2S,5R)-5-(6-amino-purin-9-yl)-4-fluoro-2,5-dihydro-furan-2-yl]-methanol.Macroheterocyclic nucleoside derivative and its analog of the general formula 1 or general formula 2, a stereoisomer, isotope-enriched analog, pharmaceutically acceptable salt, hydrate, solvate, or crystalline or polymorphic form thereof, wherein: Ar is aryl or hetaryl; R1 and R2 are not necessarily the same substituents selected from H, F, Cl, CH3, OH; R3 is H or CH3; X is oxygen or ethanediyl-1,1 (C═CH2); Y is CH(R4)(CH2)k, CH(R4)(CH2)mC(O)O(CH2)n; R4 is H or CH3; k has a value from zero to six; m has a value from zero to two; n has a value of one to four; Q is a radical selected from Q1-Q4; wherein: R5 is the substituent selected from H, F, Cl, CH3, OH; the arrow (→) indicates the location, joined by Q1-Q4.

    Macroheterocyclic nucleoside derivatives and their analogues, production and use thereof
    28.
    发明申请
    Macroheterocyclic nucleoside derivatives and their analogues, production and use thereof 审中-公开

    公开(公告)号：US20180099989A1

    公开(公告)日：2018-04-12

    申请号：US15287805

    申请日：2016-10-07

    申请人： Alexandre Vasilievich Ivachtchenko ,  Andrey Alexandrovich Ivashchenko ,  Nikolay Filippovich Savchuk ,  Alena Alexandrovna Ivachtchenko ,  Oleg Dmitrievich Mitkin ,  ASAVI, LLC

    发明人： Alexandre Vasilievich Ivachtchenko ,  Oleg Dmitrievich Mitkin ,  Andrey Alexandrovich Ivashchenko ,  Alena Alexandrovna Ivachtchenko ,  Nikolay Filippovich Savchuk

    IPC分类号： C07H19/10 ,  A61K45/06 ,  A61K31/7072

    CPC分类号： C07H19/10 ,  A61K31/7068 ,  A61K31/7072 ,  A61K31/7076 ,  A61K31/708 ,  A61K45/06 ,  A61K2300/00

    摘要： Nucleosides and nucleotides (nucleos(t)ides) have been in clinical use for almost 50 years and have become cornerstones of treatment for patients with viral infections or cancer. The approval of several additional drugs over the past decade demonstrates that this family still possesses strong potential. Therefore nucleos(t)ide are of great interest as promising chemotherapeutic agents, including: 2′-deoxy-L-uridine (CAS No 31501-19-6), 2′-deoxy-D-uridine (CAS No 951-78-0), telbivudine (CAS No 3424-98-4), zidovudine (AZT, CAS No 30516-87-1), trifluridine (CAS No 70-00-8), clevudine (CAS No 163252-36-6), PSI-6206 (CAS No 863329-66-2), 2′-(5)-2′-chloro-2′-deoxy-2′-fluorouridine (CAS No 1673560-41-2), ND06954 (CAS No 114248-23-6), stavudine (CAS No 3056-17-5), 5-ethynyltavudine (Festinavir, CAS No 634907-30-5), torcitabine (CAS No 40093-94-5), (−)-beta-D-(2R,4R)-dioxolane-thymine (DOT, 1-((2R,4R)-2-(hydroxymethyl)-1,3-dioxolan-4-yl)-5-methyl-2,4 (1H,3H)-pyrimidinedione, CAS No. 127658-07-5), 2-(6-amino-purin-9-yl)-ethanol (CAS No 707-99-3), 2′-C-methylcytidine (CAS No 20724-73-6), PSI-6130 (CAS No 817204-33-4), gemcitabine (CAS No 95058-81-4), 2′-chloro-2′-deoxy-2′-fluorocytidine (CAS No 1786426-19-4), 2′,2′-dichloro-2′-deoxycytidine (CAS No 1703785-65-2), 2′-C-methylcytidine (CAS No 20724-73-6), PSI-6130 (CAS No 817204-33-4), lamivudine (3TC, CAS No 134678-17-4), emtricitabine (CAS No 143491-57-0), 2′-deoxyadenosine (CAS No 958-09-8), 2′-deoxy-β-L-adenosine (CAS No 14365-45-8), 2′-deoxy-4′-C-ethynyl-2-fluoroadenosine (CAS No 865363-93-5), didanosine (CAS No 69655-05-6), entecavir (CAS No 209216-23-9), FMCA (CAS No 1307273-70-6), dioxolane-G (DOG, CAS No 145514-01-8), β-D-2′-deoxy-2′-(R)-fluoro-2′-β-C-methylguanosine (CAS No 817204-45-8), abacavir (ABC, CAS No 136470-78-5), dioxolane-A (DOA, CAS #145514-02-9), [(2R,4R)-4-(6-cyclopropylamino-purin-9-yl)-[1,3]dioxolan-2-yl]-methanol (CAS No 1446751-04-7), amdoxovir (AMDX, CAS No 145514-04-1), (R)-1-(6-amino-purin-9-yl)-propan-2-ol (CAS No 14047-28-0), and [(2S,5R)-5-(6-amino-purin-9-yl)-4-fluoro-2,5-dihydro-furan-2-yl]-methanol.Macroheterocyclic nucleoside derivative and its analogue of the general formula 1 or general formula 2, a stereoisomer, isotope-enriched analogue, pharmaceutically acceptable salt, hydrate, solvate, or crystalline or polymorphic form thereof, wherein: Ar is aryl or hetaryl; R1 and R2 are not necessarily the same substituents selected from H, F, Cl, CH3, OH; R3 is H or CH3; X is oxygen or ethanediyl-1,1 (C═CH2); Y is CH(R4)(CH2)k, CH(R4)(CH2)mC(O)O(CH2)n; R4 is H or CH3; k has a value from zero to six; m has a value from zero to two; n has a value of one to four; Q is a radical selected from Q1-Q4; wherein: R5 is the substituent selected from H, F, Cl, CH3, OH; the arrow (→) indicates the location, joined by Q1-Q4.