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1. 发明授权

US08334294B2 4,8-diphenyl-polyazanaphthalene derivatives 失效
标题翻译：新的4,8-二苯基 - 多氮杂萘衍生物
公开(公告)号：US08334294B2
公开(公告)日：2012-12-18
申请号：US12597187
申请日：2008-04-25
申请人： Wenceslao Lumeras Amador , Paul Robert Eastwood
发明人： Wenceslao Lumeras Amador , Paul Robert Eastwood
IPC分类号： A01N43/42 , A01N43/90 , A61K31/44 , A61K31/519
CPC分类号： C07D471/04
摘要： New inhibitors of the p38 mitogen-activated protein kinase having the general formula (I) are disclosed herein, as well as processes for their preparation, pharmaceutical compositions comprising them, and their use in therapy.
摘要翻译：本文公开了具有通式（I）的p38丝裂原活化蛋白激酶的新抑制剂，以及其制备方法，包含它们的药物组合物及其在治疗中的用途。

2. 发明申请

US20100130517A1 NEW 4,8-DIPHENYL-POLYAZANAPHTHALENE DERIVATIVES 失效
标题翻译：新的4,8-二苯基 - 二亚甲基蒽醌衍生物
公开(公告)号：US20100130517A1
公开(公告)日：2010-05-27
申请号：US12597187
申请日：2008-04-25
申请人： Wenceslao Lumeras Amador , Paul Robert Eastwood
发明人： Wenceslao Lumeras Amador , Paul Robert Eastwood
IPC分类号： A61K31/519 , A61K31/4375 , C07D471/02 , C07D471/04 , A61P19/02 , A61P25/28 , A61P19/10 , A61P11/00 , A61P9/10 , A61P11/06
CPC分类号： C07D471/04
摘要： New inhibitors of the p38 mitogen-activated protein kinase having the general formula (I) are disclosed herein, as well as processes for their preparation, pharmaceutical compositions comprising them, and their use in therapy.
摘要翻译：本文公开了具有通式（I）的p38丝裂原活化蛋白激酶的新抑制剂，以及其制备方法，包含它们的药物组合物及其在治疗中的用途。

3. 发明授权

US08258122B2 3-([1,2,4]triazolo[4,3-a]pyridin-7-yl)benzamide derivatives 有权
标题翻译： 3 - （[1,2,4]三唑并[4,3-a]吡啶-7-基）苯甲酰胺衍生物
公开(公告)号：US08258122B2
公开(公告)日：2012-09-04
申请号：US12529490
申请日：2008-02-29
申请人： Bernat Vidal Juan , Paul Robert Eastwood , Jacob Gonzalez Rodriguez , Cristina Esteve Trias
发明人： Bernat Vidal Juan , Paul Robert Eastwood , Jacob Gonzalez Rodriguez , Cristina Esteve Trias
IPC分类号： A61K31/56 , A61K31/437 , A61K31/5377 , A61K31/506 , C07D471/04 , C07D413/14 , C07D401/14 , A61P37/02 , A61P19/02 , A61P25/00 , A61P9/00 , A61P1/00
CPC分类号： C07D471/04
摘要： New inhibitors of the p38 mitogen-activated protein kinase having the general formula (I) are disclosed herein, as well as processes for their preparation, pharmaceutical compositions comprising them, and their use in therapy.
摘要翻译：本文公开了具有通式（I）的p38丝裂原活化蛋白激酶的新抑制剂，以及其制备方法，包含它们的药物组合物及其在治疗中的用途。

4. 发明授权

US08008491B2 Substituted AZA-indoles as inhibitors of poly(ADP-ribose) polymerase (PARP) 失效
标题翻译：取代的AZA-吲哚作为聚（ADP-核糖）聚合酶（PARP）的抑制剂，
公开(公告)号：US08008491B2
公开(公告)日：2011-08-30
申请号：US12140632
申请日：2008-06-17
申请人： John Ziqi Jiang , Jack Roger Koehl , Shujaath Mehdi , Neil Moorcroft , Kwon Yon Musick , Philip Marvin Weintraub , Paul Robert Eastwood
发明人： John Ziqi Jiang , Jack Roger Koehl , Shujaath Mehdi , Neil Moorcroft , Kwon Yon Musick , Philip Marvin Weintraub , Paul Robert Eastwood
IPC分类号： C07D403/04 , C07D209/04
CPC分类号： C04B35/632 , A61K31/404 , A61K31/454 , A61K31/4745 , A61K31/496 , A61K31/503 , A61K31/5377 , A61K31/541 , A61K31/55 , C07D209/40 , C07D401/04 , C07D401/10 , C07D401/12 , C07D403/04 , C07D403/10 , C07D405/12 , C07D405/14 , C07D409/04 , C07D471/04 , C07D487/08
摘要： The present invention relates to a series of substituted aza-indole derivatives of the formula I: wherein R, R1, R2, R3, R4, X and Y are as defined herein. This invention also relates to methods of making these compounds. The compounds of this invention are inhibitors of poly(adenosine 5′-diphosphate ribose) polymerase (PARP) and are therefore useful as pharmaceutical agents, especially in the treatment and/or prevention of a variety of diseases, including diseases associated with the central nervous system and cardiovascular disorders.
摘要翻译：本发明涉及一系列式I的取代的氮杂 - 吲哚衍生物：其中R，R 1，R 2，R 3，R 4，X和Y如本文所定义。本发明还涉及制备这些化合物的方法。本发明的化合物是聚（腺苷5'-二磷酸核糖）聚合酶（PARP）的抑制剂，因此可用作药剂，特别是用于治疗和/或预防各种疾病，包括与中枢神经相关的疾病系统和心血管疾病。

5. 发明申请

US20140271543A1 PYRIDIN-2(1H)-ONE DERIVATIVES AS JAK INHIBITORS 有权
标题翻译：吡啶-2（1H） - 酮衍生物作为JAK抑制剂
公开(公告)号：US20140271543A1
公开(公告)日：2014-09-18
申请号：US14236340
申请日：2012-07-23
申请人： Paul Robert Eastwood , Jordi Bach Taña , Lluis Miquel Pages Santacana
发明人： Paul Robert Eastwood , Jordi Bach Taña , Lluis Miquel Pages Santacana
IPC分类号： C07D413/14 , A61K31/506 , A61K31/5377 , A61K31/56 , C07D401/04 , C07D409/14 , A61K45/06 , A61K38/21 , C07D401/14 , A61K31/444
CPC分类号： C07D413/14 , A61K31/444 , A61K31/506 , A61K31/5377 , A61K31/56 , A61K38/212 , A61K38/215 , A61K45/06 , C07D401/04 , C07D401/12 , C07D401/14 , C07D409/14
摘要： New pyridin-2(1H)-one derivatives having the chemical structure of formula (I) are disclosed; as well as process for their preparation, pharmaceutical compositions comprising them and their use in therapy as inhibitors of Janus Kinases (JAK).
摘要翻译：公开了具有式（I）化学结构的新的吡啶-2（1H） - 酮衍生物; 以及其制备方法，包含它们的药物组合物及其在治疗中作为Janus Kinases（JAK）抑制剂的用途。

6. 发明授权

US08772288B2 Substituted spiro[cycloalkyl-1,3′-indo]-2′(1′H)-one derivatives and their use as P38 mitogen-activated kinase inhibitors 失效
标题翻译：取代的螺[环烷基-1,3'-吲哚] -2'（1'H） - 酮衍生物及其作为P38丝裂原活化激酶抑制剂的用途
公开(公告)号：US08772288B2
公开(公告)日：2014-07-08
申请号：US12936784
申请日：2009-04-03
申请人： Paul Robert Eastwood , Jacob Gonzalez Rodriguez , Bernet Vidal Juan , Nuria Aguilar Izquierdo
发明人： Paul Robert Eastwood , Jacob Gonzalez Rodriguez , Bernet Vidal Juan , Nuria Aguilar Izquierdo
IPC分类号： A61K31/403 , A61K31/4178 , A61K31/4196 , A61K31/4245 , A61K31/438 , A61K31/519 , A61K31/5377 , A61K31/4439 , A61K31/437 , A61P29/00 , A61P1/00 , A61P9/00 , A61P17/06 , C07D403/10 , C07D209/96 , C07D413/10 , C07D413/14 , C07D471/10 , C07D487/04 , C07D491/20 , C07D491/107 , C07D495/10 , C07D487/10
CPC分类号： C07D209/34 , C07D209/96
摘要： The present disclosure is directed to new inhibitors of the p38 mitogen-activated protein kinase having the general formula (I), processes for preparation thereof, pharmaceutical compositions thereof, and methods of use thereof.
摘要翻译：本公开涉及具有通式（I）的p38丝裂原活化蛋白激酶的新抑制剂，其制备方法，其药物组合物及其使用方法。

7. 发明申请

US20140086870A9 PYRAZOLE DERIVATIVES AS JAK INHIBITORS 有权
标题翻译：吡唑衍生物作为JAK抑制剂
公开(公告)号：US20140086870A9
公开(公告)日：2014-03-27
申请号：US13579344
申请日：2011-02-18
申请人： Jordi Bach Taña , Lluis Miquel Pages Santacana , Joan Taltavull Moll , Paul Robert Eastwood , Jacob Gonzalez Rodrigues , Victor Giulio Matassa
发明人： Jordi Bach Taña , Lluis Miquel Pages Santacana , Joan Taltavull Moll , Paul Robert Eastwood , Jacob Gonzalez Rodrigues , Victor Giulio Matassa
IPC分类号： C07D471/04 , A61K45/06 , A61K31/4985 , A61K31/497 , A61K31/506 , C07D487/04
CPC分类号： C07D487/04 , A61K31/437 , A61K31/497 , A61K31/4985 , A61K31/506 , A61K45/06 , C07D471/04
摘要： New pyrazole derivatives having the chemical structure of formula (I) are disclosed; as well as process for their preparation, pharmaceutical compositions comprising them and their use in therapy as inhibitors of Janus Kinases (JAK).
摘要翻译：公开了具有式（I）化学结构的新的吡唑衍生物; 以及其制备方法，包含它们的药物组合物及其在治疗中作为Janus Kinases（JAK）抑制剂的用途。

8. 发明申请

US20080275038A1 Imidazopyridine Derivatives as A2b Adenosine Receptor Antagonists 失效
标题翻译：咪唑并吡啶衍生物作为A2b腺苷受体拮抗剂
公开(公告)号：US20080275038A1
公开(公告)日：2008-11-06
申请号：US12089050
申请日：2006-10-05
申请人： Bernat Vidal Juan , Silvia Fonquerna Pou , Paul Robert Eastwood , Jose Aiguade Bosch , Aranzazu Cardus Figueras , Ines Carranco Moruno , Jacob Gonzalez Rodriguez , Sergio Paredes Aparicio
发明人： Bernat Vidal Juan , Silvia Fonquerna Pou , Paul Robert Eastwood , Jose Aiguade Bosch , Aranzazu Cardus Figueras , Ines Carranco Moruno , Jacob Gonzalez Rodriguez , Sergio Paredes Aparicio
IPC分类号： A61K31/437 , A61P11/00 , A61P1/00 , A61P9/00 , A61P25/00 , A61P37/00 , C07D471/04 , A61K31/506 , A61K31/5377 , A61K31/496 , A61K31/497
CPC分类号： C07D471/04
摘要： The present disclosure relates to imidazopyridine derivatives of formula (I): The present disclosure also relates to a method for treating a subject afflicted with a pathological condition or disease susceptible to amelioration by antagonism of the A2B adenosine receptor.
摘要翻译：本公开内容涉及式（I）的咪唑并吡啶衍生物：本公开还涉及用于治疗受到Aβ拮抗作用而易于改善的病理状况或疾病的受试者的治疗方法。

9. 发明授权

US06620832B2 Substituted ureas 有权
标题翻译：取代尿素
公开(公告)号：US06620832B2
公开(公告)日：2003-09-16
申请号：US10002747
申请日：2001-11-02
申请人： Paul Robert Eastwood
发明人： Paul Robert Eastwood
IPC分类号： A61K3140
CPC分类号： C07D401/12 , C07D209/08
摘要： The invention is directed to physiologically active compounds of general formula (I): wherein R1 is lower alkyl, R2 is aryl, arylalkyl, heteroaryl or heteroarylalkyl, or R1 and R2 together with the nitrogen atom to which they are attached form a cyclic amine, Ar1 is aryldiyl or heteroaryldiyl, Ar2 is optionally substituted phenylene or heteroaryldiyl, L1 is an a —R5—R6— linkage where R5 is alkylene, alkenylene or alkynylene and R6 is a direct bond, cycloalkylene, heterocycloalkylene, arylene, heteroaryldiyl, —C(═Z1)—NR4—, —NR4—C(═Z1)—, —Z1—, —C(═O)—, —C(═NOR4)—, —NR4—, —NR4—C(═Z1)—NR4—, —SO2—NR4—, —NR4—SO2—, —O—C(═O)—, —C(═O)—O—, —NR4—C(═O)—O— or —O—C(═O)—NR4—, L2 is a direct bond, an optionally substituted alkylene, alkenylene, alkynylene, cycloalkenylene, cycloalkylene, heteroaryldiyl, heterocycloalkylene or aryldiyl linkage, a —[C(═O)—N(R9)—C(R4)(R10)]p— linkage, a —Z3—R11— linkage, a —C(═O)—CH2—C(═O)— linkage or a —R11—Z3—R11— linkage, and Y is carboxy or an acid bioisostere; and the corresponding N-oxides, and their prodrugs; and pharmaceutically acceptable salts and solvates (e.g. hydrates) of such compounds and their N-oxides and prodrugs. Such compounds have valuable pharmaceutical properties, in particular the ability to regulate the interaction of VCAM-1 and fibronectin with the integrin VLA-4 (&agr;4&bgr;1).
摘要翻译：本发明涉及通式（I）的生理活性化合物：其中R 1是低级烷基，R 2是芳基，芳烷基，杂芳基或杂芳基烷基，或者R 1和R 2与它们所连接的氮原子一起形成环状胺， Ar 1是芳基或杂芳基二，Ar 2是任选取代的亚苯基或杂芳基二基，L1是一个-R5-R6-键，其中R5是亚烷基，亚烯基或亚炔基，R6是直接键，亚环烷基，亚杂环亚烷基，亚芳基，杂芳基二基，-C（ = Z1）-NR4-，-NR4-C（= Z1） - ，-Z1，-C（= O） - ， - （= NOR4） - ，-NR4-，-NR4-C（= NR4-，-SO2-NR4-，-NR4-SO2-，-OC（= O） - ， - C（= O）-O-，-NR4-C（= O）-O-或-OC ） - NR 4 - ，L 2是直接键，任选取代的亚烷基，亚烯基，亚炔基，亚环烯基，亚环烷基，杂芳基二基，杂环亚烷基或芳基二键，a- [C（= O）-N（R 9）-C（R 4） R 10）] p键，-Z 3 -R 11键，-C（= O）-CH 2 -C（= O） - 键或-R 11 -Z 3 -R 11键，Y是羧基或酸生物电子和相应的N-氧化物及其前药; 和这些化合物的药学上可接受的盐和溶剂合物（例如水合物）及其N-氧化物和前药。这些化合物具有有价值的药物性质，特别是调节VCAM-1和纤连蛋白与整联蛋白VLA-4（α4β1 ）。

10. 发明申请

US20140170110A1 PYRIDIN-2(1H)-ONE DERIVATIVES USEFUL AS MEDICAMENTS FOR THE TREATMENT OF MYELOPROLIFERATIVE DISORDERS, TRANSPLANT REJECTION, IMMUNE-MEDIATED AND INFLAMMATORY DISEASES 审中-公开
标题翻译：吡哩啶-2（1H） - 酮衍生物有助于治疗失语性疾病的药物，移植物免疫，免疫介导和炎症疾病
公开(公告)号：US20140170110A1
公开(公告)日：2014-06-19
申请号：US14119920
申请日：2012-05-21
申请人： Paul Robert Eastwood , Jacob Gonzalez Rodriguez , Elena Gomez Castillo , Jordi Bach Taña
发明人： Paul Robert Eastwood , Jacob Gonzalez Rodriguez , Elena Gomez Castillo , Jordi Bach Taña
IPC分类号： C07D473/28 , A61K45/06 , A61K31/444 , A61K31/5377 , A61K31/522 , C07D471/04
CPC分类号： C07D473/28 , A61K31/444 , A61K31/522 , A61K31/5377 , A61K45/06 , C07D471/02 , C07D471/04 , C07D473/00
摘要： Compounds having the chemical structure of formula (I) are disclosed; as well as process for their preparation, pharmaceutical compositions comprising them and their use in therapy as inhibitors of Janus Kinases (JAK).
摘要翻译：公开了具有式（I）化学结构的化合物; 以及其制备方法，包含它们的药物组合物及其在治疗中作为Janus Kinases（JAK）抑制剂的用途。

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