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1. 发明申请

US20140294870A1 Autoimmune and Inflammatory Disorder Therapy 有权
标题翻译：自身免疫和炎症性疾病治疗
公开(公告)号：US20140294870A1
公开(公告)日：2014-10-02
申请号：US14343416
申请日：2012-09-07
申请人： Jean Herman , Thierry Louat , Qiuya Huang , Bart Vanderhoydonck , Mark Waer , Piet Herdewijn
发明人： Jean Herman , Thierry Louat , Qiuya Huang , Bart Vanderhoydonck , Mark Waer , Piet Herdewijn
IPC分类号： A61K31/5377 , A61K31/519 , G01N33/573 , A61K31/426
CPC分类号： A61K31/5377 , A61K31/426 , A61K31/519 , G01N33/564 , G01N33/573 , G01N2333/91215 , G01N2500/02
摘要： Compounds that bind to phosphatidylinositol-4-kinase IIIβ (PI4KIIIβ) and inhibit the binding of PI4KIIIβ to its substrate and/or inhibit PI4KIIIβ activity may be used in the treatment and/or prevention of an autoimmune or inflammatory disorder, or organ or cell transplant rejection. A new assay for identifying compounds for use in treating and/or preventing those pathological conditions, which comprises measuring the inhibition of PI4KIIIβ activity, is also disclosed.
摘要翻译：结合磷脂酰肌醇-4-激酶III和bgr的化合物（PI4KIII＆bgr），并抑制PI4KIII和bgr的结合; 到其底物和/或抑制PI4KIII和bgr; 活性可用于治疗和/或预防自身免疫性或炎性疾病或器官或细胞移植排斥反应。用于鉴定用于治疗和/或预防这些病理状况的化合物的新测定法，其包括测量PI4KIII和bgr的抑制; 活动也被披露。

2. 发明申请

US20140309222A1 Therapeutically Active Fused Pyrimidine Derivatives 有权
标题翻译：治疗活性融合嘧啶衍生物
公开(公告)号：US20140309222A1
公开(公告)日：2014-10-16
申请号：US14239406
申请日：2012-08-15
申请人： Daniel Christopher Brookings , Daniel James Ford , Anant Ramrao Ghawalkar , Jean Herman , Qiuya Huang , Claire Louise Kulisa , Thierry Louat , Judi Charlotte Neuss , James Thomas Reuberson , Bart Vanderhoydonck
发明人： Daniel Christopher Brookings , Daniel James Ford , Anant Ramrao Ghawalkar , Jean Herman , Qiuya Huang , Claire Louise Kulisa , Thierry Louat , Judi Charlotte Neuss , James Thomas Reuberson , Bart Vanderhoydonck
IPC分类号： C07D495/04 , C07D513/04
CPC分类号： C07D495/04 , A61K31/519 , C07D513/04 , C07D519/00
摘要： A series of monocyclic or bicyclic diamine-substituted thieno[2,3-d]pyrimidine and isothiazolo[5,4-d]pyrimidine derivatives are beneficial in the treatment and/or prevention of various human ailments, including inflammatory, autoimmune and oncological disorders; viral diseases; and organ and cell transplant rejection.
摘要翻译：一系列单环或双环二胺取代的噻吩并[2,3-d]嘧啶和异噻唑并[5,4-d]嘧啶衍生物有助于治疗和/或预防各种人类疾病，包括炎症，自身免疫和肿瘤疾病 ; 病毒性疾病和器官和细胞移植排斥反应。

3. 发明授权

US09301961B2 Autoimmune and inflammatory disorder therapy 有权
标题翻译：自身免疫性和炎症性疾病治疗
公开(公告)号：US09301961B2
公开(公告)日：2016-04-05
申请号：US14343416
申请日：2012-09-07
申请人： Jean Herman , Thierry Louat , Qiuya Huang , Bart Vanderhoydonck , Mark Waer , Piet Herdewijn
发明人： Jean Herman , Thierry Louat , Qiuya Huang , Bart Vanderhoydonck , Mark Waer , Piet Herdewijn
IPC分类号： A61K31/426 , G01N33/564 , A61K31/5377 , A61K31/519 , G01N33/573
CPC分类号： A61K31/5377 , A61K31/426 , A61K31/519 , G01N33/564 , G01N33/573 , G01N2333/91215 , G01N2500/02
摘要： Compounds that bind to phosphatidylinositol-4-kinase IIIβ (PI4KIIIβ) and inhibit the binding of PI4KIIIβ to its substrate and/or inhibit PI4KIIIβ activity may be used in the treatment and/or prevention of an autoimmune or inflammatory disorder, or organ or cell transplant rejection. A new assay for identifying compounds for use in treating and/or preventing those pathological conditions, which comprises measuring the inhibition of PI4KIIIβ activity, is also disclosed.
摘要翻译：结合磷脂酰肌醇-4-激酶III和bgr的化合物（PI4KIII＆bgr），并抑制PI4KIII和bgr的结合; 到其底物和/或抑制PI4KIII和bgr; 活性可用于治疗和/或预防自身免疫性或炎性疾病或器官或细胞移植排斥反应。用于鉴定用于治疗和/或预防这些病理状况的化合物的新测定法，其包括测量PI4KIII和bgr的抑制; 活动也被披露。

4. 发明申请

US20160030447A1 Antiviral Activity of Novel Bicyclic Heterocycles 有权
标题翻译：新型双环杂环的抗病毒活性
公开(公告)号：US20160030447A1
公开(公告)日：2016-02-04
申请号：US14884997
申请日：2015-10-16
申请人： Steven De Jonghe , Ling-Jie Gao , Piet Herdewijn , Jean Herman , Miyeon Jang , Pieter Leyssen , Thierry Louat , Johan Neyts , Christophe Pannecouque , Bart Vanderhoydonck
发明人： Steven De Jonghe , Ling-Jie Gao , Piet Herdewijn , Jean Herman , Miyeon Jang , Pieter Leyssen , Thierry Louat , Johan Neyts , Christophe Pannecouque , Bart Vanderhoydonck
IPC分类号： A61K31/551 , A61K31/5377 , A61K31/519
CPC分类号： A61K31/551 , A61K31/519 , A61K31/52 , A61K31/5377 , C07D473/00 , C07D513/04 , Y02A50/385 , Y02A50/465
摘要： The present invention relates to compound of Formula I, II, III, or IV, and/or a pharmaceutical acceptable addition salt thereof and/or a stereoisomer thereof and/or a solvate thereof, wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, R11, and R12 are as defined in the claim 1 or as described in detail in the description of the invention, and to the use of said compounds to treat or prevent viral infections and their use to manufacture a medicine to treat or prevent viral infections, particularly infections with RNA-viruses belonging to the family of the Retroviridae, the family of the Flaviviridae and the family of the Picornaviridae and more preferably infections with Human Immunodeficiency Virus 1 (HIV1), Human Immunodeficiency Virus 2 (HN2), Hepatitis C virus (HCV), Dengue virus, and enteroviruses like Coxsackievirus, Rhinovirus and Poliovirus. The present invention also relates to pharmaceutical compositions of said compounds and the use of said pharmaceutical compositions to treat or prevent viral infections. The present invention further relates to the use of said compounds as biologically active ingredients, more specifically as medicaments for the treatment of viral disorders and pathologic conditions such as, but not limited to, viral infections with Human Immunodeficiency Virus 1 (HIV1), Human Immunodeficiency Virus 2 (HN2), Hepatitis C virus (HCV), Dengue virus, and enteroviruses like Coxsackievirus, Rhinovirus and Poliovints.
摘要翻译：本发明涉及式I，II，III或IV化合物和/或其药学上可接受的加成盐和/或其立体异构体和/或其溶剂合物，其中R1，R2，R3，R4，R5， R6，R7，R8，R9，R11和R12如权利要求1中所定义或如在本发明的描述中详细描述的，以及所述化合物用于治疗或预防病毒感染及其用于制造治疗或预防病毒感染的药物，特别是属于逆转录病毒科的家族，微病毒科的家族和小核糖核酸病毒科家族的RNA病毒的感染，更优选人免疫缺陷病毒1（HIV1），人类免疫缺陷病毒2 （HN2），丙型肝炎病毒（HCV），登革热病毒和诸如柯萨奇病毒，鼻病毒和脊髓灰质炎病毒的肠道病毒。本发明还涉及所述化合物的药物组合物和所述药物组合物用于治疗或预防病毒感染的用途。本发明还涉及所述化合物作为生物活性成分的用途，更具体地说，作为治疗病毒性病症和病理状况的药物，例如但不限于人免疫缺陷病毒1（HIV1），人类免疫缺陷病毒病毒2（HN2），丙型肝炎病毒（HCV），登革热病毒和诸如柯萨奇病毒，鼻病毒和Poliovints的肠道病毒。

5. 发明授权

US09227984B2 Therapeutically active fused pyrimidine derivatives 有权
标题翻译：治疗活性的融合嘧啶衍生物
公开(公告)号：US09227984B2
公开(公告)日：2016-01-05
申请号：US14239406
申请日：2012-08-15
申请人： Daniel Christopher Brookings , Daniel James Ford , Anant Ramrao Ghawalkar , Jean Herman , Qiuya Huang , Claire Louise Kulisa , Thierry Louat , Judi Charlotte Neuss , James Thomas Reuberson , Bart Vanderhoydonck
发明人： Daniel Christopher Brookings , Daniel James Ford , Anant Ramrao Ghawalkar , Jean Herman , Qiuya Huang , Claire Louise Kulisa , Thierry Louat , Judi Charlotte Neuss , James Thomas Reuberson , Bart Vanderhoydonck
IPC分类号： A01N43/90 , A61K31/519 , C07D471/00 , C07D487/00 , C07D491/00 , C07D495/04 , C07D513/04 , C07D519/00
CPC分类号： C07D495/04 , A61K31/519 , C07D513/04 , C07D519/00
摘要： A series of monocyclic or bicyclic diamine-substituted thieno[2,3-d]pyrimidine and isothiazolo[5,4-d]pyrimidine derivatives are beneficial in the treatment and/or prevention of various human ailments, including inflammatory, autoimmune and oncological disorders; viral diseases; and organ and cell transplant rejection.
摘要翻译：一系列单环或双环二胺取代的噻吩并[2,3-d]嘧啶和异噻唑并[5,4-d]嘧啶衍生物有助于治疗和/或预防各种人类疾病，包括炎症，自身免疫和肿瘤疾病 ; 病毒性疾病和器官和细胞移植排斥反应。

6. 发明授权

US09730944B2 Antiviral activity of novel bicyclic heterocycles 有权
公开(公告)号：US09730944B2
公开(公告)日：2017-08-15
申请号：US14884997
申请日：2015-10-16
申请人： Steven De Jonghe , Ling-Jie Gao , Piet Herdewijn , Jean Herman , Miyeon Jang , Pieter Leyssen , Thierry Louat , Johan Neyts , Christophe Pannecouque , Bart Vanderhoydonck
发明人： Steven De Jonghe , Ling-Jie Gao , Piet Herdewijn , Jean Herman , Miyeon Jang , Pieter Leyssen , Thierry Louat , Johan Neyts , Christophe Pannecouque , Bart Vanderhoydonck
IPC分类号： C07D473/00 , A61K31/52 , A61K31/551 , A61K31/519 , C07D513/04 , A61K31/5377
CPC分类号： A61K31/551 , A61K31/519 , A61K31/52 , A61K31/5377 , C07D473/00 , C07D513/04 , Y02A50/385 , Y02A50/465
摘要： The present invention relates to compound of Formula I, II, III, or IV, and/or a pharmaceutical acceptable addition salt thereof and/or a stereoisomer thereof and/or a solvate thereof, wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, R11, and R12 are as defined in the claim 1 or as described in detail in the description of the invention, and to the use of said compounds to treat or prevent viral infections and their use to manufacture a medicine to treat or prevent viral infections, particularly infections with RNA-viruses belonging to the family of the Retroviridae, the family of the Flaviviridae and the family of the Picornaviridae and more preferably infections with Human Immunodeficiency Virus 1 (HIV1), Human Immunodeficiency Virus 2 (HIV2), Hepatitis C virus (HCV), Dengue virus, and enteroviruses like Coxsackievirus, Rhinovirus and Poliovirus. The present invention also relates to pharmaceutical compositions of said compounds and the use of said pharmaceutical compositions to treat or prevent viral infections. The present invention further relates to the use of said compounds as biologically active ingredients, more specifically as medicaments for the treatment of viral disorders and pathologic conditions such as, but not limited to, viral infections with Human Immunodeficiency Virus 1 (HIV1), Human Immunodeficiency Virus 2 (HIV2), Hepatitis C virus (HCV), Dengue virus, and enteroviruses like Coxsackievirus, Rhinovirus and Poliovints.

7. 发明授权

US09193741B2 Antiviral activity of bicyclic heterocycles 有权
标题翻译：双环杂环的抗病毒活性
公开(公告)号：US09193741B2
公开(公告)日：2015-11-24
申请号：US13699258
申请日：2011-05-20
申请人： Steven De Jonghe , Ling-Jie Gao , Piet Herdewijn , Jean Herman , Miyeon Jang , Pieter Leyssen , Thierry Louat , Johan Neyts , Christophe Pannecouque , Bart Vanderhoydonck
发明人： Steven De Jonghe , Ling-Jie Gao , Piet Herdewijn , Jean Herman , Miyeon Jang , Pieter Leyssen , Thierry Louat , Johan Neyts , Christophe Pannecouque , Bart Vanderhoydonck
IPC分类号： A61K31/519 , C07D513/04 , A61K31/52 , A61K31/551
CPC分类号： A61K31/551 , A61K31/519 , A61K31/52 , A61K31/5377 , C07D473/00 , C07D513/04 , Y02A50/385 , Y02A50/465
摘要： The present invention relates to compound of Formula I, II, III, or IV, and/or a pharmaceutical acceptable addition salt thereof and/or a stereoisomer thereof and/or a solvate thereof, wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, R11, and R12 are as defined in the claim 1 or as described in detail in the description of the invention, and to the use of said compounds to treat or prevent viral infections and their use to manufacture a medicine to treat or prevent viral infections, particularly infections with RNA-viruses belonging to the family of the Retroviridae, the family of the Flaviviridae and the family of the Picornaviridae and more preferably infections with Human Immunodeficiency Virus 1 (HIV1), Human Immunodeficiency Virus 2 (HIV2), Hepatitis C virus (HCV), Dengue virus, and enteroviruses like Coxsackievirus, Rhinovirus and Poliovirus. The present invention also relates to pharmaceutical compositions of said compounds and the use of said pharmaceutical compositions to treat or prevent viral infections. The present invention further relates to the use of said compounds as biologically active ingredients, more specifically as medicaments for the treatment of viral disorders and pathologic conditions such as, but not limited to, viral infections with Human Immunodeficiency Virus 1 (HIV1), Human Immunodeficiency Virus 2 (HIV2), Hepatitis C virus (HCV), Dengue virus, and enteroviruses like Coxsackievirus, Rhinovirus and Poliovirus.
摘要翻译：本发明涉及式I，II，III或IV化合物和/或其药学上可接受的加成盐和/或其立体异构体和/或其溶剂合物，其中R1，R2，R3，R4，R5， R6，R7，R8，R9，R11和R12如权利要求1中所定义或如在本发明的描述中详细描述的，以及所述化合物用于治疗或预防病毒感染及其用于制造治疗或预防病毒感染的药物，特别是属于逆转录病毒科的家族，微病毒科的家族和小核糖核酸病毒科家族的RNA病毒的感染，更优选人免疫缺陷病毒1（HIV1），人类免疫缺陷病毒2 （HIV2），丙型肝炎病毒（HCV），登革热病毒和诸如柯萨奇病毒，鼻病毒和脊髓灰质炎病毒的肠道病毒。本发明还涉及所述化合物的药物组合物和所述药物组合物用于治疗或预防病毒感染的用途。本发明还涉及所述化合物作为生物活性成分的用途，更具体地说，作为治疗病毒性病症和病理状况的药物，例如但不限于人免疫缺陷病毒1（HIV1），人类免疫缺陷病毒病毒2（HIV2），丙型肝炎病毒（HCV），登革热病毒和诸如柯萨奇病毒，鼻病毒和脊髓灰质炎病毒的肠道病毒。

8. 发明申请

US20150038494A1 Thiazolopyrimidine Modulators as Immunosuppressive Agents 有权
标题翻译：噻唑并嘧啶调节剂作为免疫抑制剂
公开(公告)号：US20150038494A1
公开(公告)日：2015-02-05
申请号：US14518480
申请日：2014-10-20
申请人： Piet Herdewijn , Steven De Jonghe , Ling-Jie Gao , Mi-Yeon Jang , Bart Vanderhoydonck , Mark Jozef Albert Waer , Yuan Lin , Jean Ferdinand Herman , Thierry Andre Michel Louat
发明人： Piet Herdewijn , Steven De Jonghe , Ling-Jie Gao , Mi-Yeon Jang , Bart Vanderhoydonck , Mark Jozef Albert Waer , Yuan Lin , Jean Ferdinand Herman , Thierry Andre Michel Louat
IPC分类号： C07D473/32 , A61K31/5513 , C07D473/18 , A61K31/5377 , A61K31/517 , A61K45/06
CPC分类号： C07D473/32 , A61K31/517 , A61K31/519 , A61K31/5377 , A61K31/5513 , A61K45/06 , C07D473/18 , C07D513/04
摘要： The present invention relates to compound of formula I, II, III, or IV, and/or a pharmaceutical acceptable addition salt thereof and/or a stereoisomer thereof and/or a solvate thereof, wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, R11, and R12 are as defined in the claim 1. The present invention also relates to a method for their preparation, as well as to pharmaceutical compositions thereof. The present invention further relates to the use of said compounds as biologically active ingredients, more specifically as medicaments for the treatment of disorders and pathologic conditions such as, but not limited to, immune and auto-immune disorders, organ and cells transplant rejections.
摘要翻译：本发明涉及式I，II，III或IV化合物和/或其药学上可接受的加成盐和/或其立体异构体和/或其溶剂合物，其中R1，R2，R3，R4，R5， R6，R7，R8，R9，R11和R12如权利要求1中所定义。本发明还涉及其制备方法及其药物组合物。本发明还涉及所述化合物作为生物活性成分的用途，更具体地说，作为用于治疗疾病和病理状况的药物，例如但不限于免疫和自身免疫病症，器官和细胞移植排斥。

9. 发明授权

US08901132B2 Thiazolopyrimidine modulators as immunosuppressive agents 有权
标题翻译：噻唑并嘧啶调节剂作为免疫抑制剂
公开(公告)号：US08901132B2
公开(公告)日：2014-12-02
申请号：US13255429
申请日：2010-03-15
申请人： Piet Herdewijn , Steven De Jonghe , Ling-Jie Gao , Mi-Yeon Jang , Bart Vanderhoydonck , Mark Jozef Albert Waer , Yuan Lin , Jean Ferdinand Herman , Thierry Andre Michel Louat
发明人： Piet Herdewijn , Steven De Jonghe , Ling-Jie Gao , Mi-Yeon Jang , Bart Vanderhoydonck , Mark Jozef Albert Waer , Yuan Lin , Jean Ferdinand Herman , Thierry Andre Michel Louat
IPC分类号： A61K31/519 , C07D495/02 , C07D513/22 , C07D513/04
CPC分类号： C07D473/32 , A61K31/517 , A61K31/519 , A61K31/5377 , A61K31/5513 , A61K45/06 , C07D473/18 , C07D513/04
摘要： The present invention relates to compound of formula I, II, III, or IV, and/or a pharmaceutical acceptable addition salt thereof and/or a stereoisomer thereof and/or a solvate thereof, wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, R11, and R12 are as defined in the claim 1. The present invention also relates to a method for their preparation, as well as to pharmaceutical compositions thereof. The present invention further relates to the use of said compounds as biologically active ingredients, more specifically as medicaments for the treatment of disorders and pathologic conditions such as, but not limited to, immune and auto-immune disorders, organ and cells transplant rejections.
摘要翻译：本发明涉及式I，II，III或IV化合物和/或其药学上可接受的加成盐和/或其立体异构体和/或其溶剂合物，其中R1，R2，R3，R4，R5， R6，R7，R8，R9，R11和R12如权利要求1中所定义。本发明还涉及其制备方法及其药物组合物。本发明还涉及所述化合物作为生物活性成分的用途，更具体地说，作为用于治疗疾病和病理状况的药物，例如但不限于免疫和自身免疫病症，器官和细胞移植排斥。

10. 发明申请

US20130190297A1 Antiviral Activity of Novel Bicyclic Heterocycles 有权
标题翻译：新型双环杂环的抗病毒活性
公开(公告)号：US20130190297A1
公开(公告)日：2013-07-25
申请号：US13699258
申请日：2011-05-20
申请人： Steven De Jonghe , Ling-Jie Gao , Piet Herdewijn , Jean Herman , Miyeon Jang , Pieter Leyssen , Thierry Louat , Johan Neyts , Christophe Pannecouque , Bart Vanderhoydonck
发明人： Steven De Jonghe , Ling-Jie Gao , Piet Herdewijn , Jean Herman , Miyeon Jang , Pieter Leyssen , Thierry Louat , Johan Neyts , Christophe Pannecouque , Bart Vanderhoydonck
IPC分类号： C07D513/04
CPC分类号： A61K31/551 , A61K31/519 , A61K31/52 , A61K31/5377 , C07D473/00 , C07D513/04 , Y02A50/385 , Y02A50/465
摘要： The present invention relates to compound of Formula I, II, III, or IV, and/or a pharmaceutical acceptable addition salt thereof and/or a stereoisomer thereof and/or a solvate thereof, wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, R11, and R12 are as defined in the claim 1 or as described in detail in the description of the invention, and to the use of said compounds to treat or prevent viral infections and their use to manufacture a medicine to treat or prevent viral infections, particularly infections with RNA-viruses belonging to the family of the Retroviridae, the family of the Flaviviridae and the family of the Picornaviridae and more preferably infections with Human Immunodeficiency Virus 1 (HIV1), Human Immunodeficiency Virus 2 (HIV2), Hepatitis C virus (HCV), Dengue virus, and enteroviruses like Coxsackievirus, Rhinovirus and Poliovirus. The present invention also relates to pharmaceutical compositions of said compounds and the use of said pharmaceutical compositions to treat or prevent viral infections. The present invention further relates to the use of said compounds as biologically active ingredients, more specifically as medicaments for the treatment of viral disorders and pathologic conditions such as, but not limited to, viral infections with Human Immunodeficiency Virus 1 (HIV1), Human Immunodeficiency Virus 2 (HIV2), Hepatitis C virus (HCV), Dengue virus, and enteroviruses like Coxsackievirus, Rhinovirus and Poliovirus.
摘要翻译：本发明涉及式I，II，III或IV化合物和/或其药学上可接受的加成盐和/或其立体异构体和/或其溶剂合物，其中R1，R2，R3，R4，R5， R6，R7，R8，R9，R11和R12如权利要求1中所定义或如在本发明的描述中详细描述的，以及所述化合物用于治疗或预防病毒感染及其用于制造治疗或预防病毒感染的药物，特别是属于逆转录病毒科的家族，微病毒科的家族和小核糖核酸病毒科家族的RNA病毒的感染，更优选人免疫缺陷病毒1（HIV1），人类免疫缺陷病毒2 （HIV2），丙型肝炎病毒（HCV），登革热病毒和诸如柯萨奇病毒，鼻病毒和脊髓灰质炎病毒的肠道病毒。本发明还涉及所述化合物的药物组合物和所述药物组合物用于治疗或预防病毒感染的用途。本发明还涉及所述化合物作为生物活性成分的用途，更具体地说，作为治疗病毒性病症和病理状况的药物，例如但不限于人免疫缺陷病毒1（HIV1），人类免疫缺陷病毒病毒2（HIV2），丙型肝炎病毒（HCV），登革热病毒和诸如柯萨奇病毒，鼻病毒和脊髓灰质炎病毒的肠道病毒。

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