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1. 发明专利

IL246614A (2s)-n-[(1s)-1-cyano-2-phenylethyl]-1,4-oxazepane-2-carboxamides as dipeptidyl peptidase inhibitors 未知
公开(公告)号：IL246614A
公开(公告)日：2018-02-28
申请号：IL24661416
申请日：2016-07-05
申请人： ASTRAZENECA AB , HANS ROLAND LONN , STEPHEN CONNOLLY , STEVEN SWALLOW , STAFFAN PO KARLSSON , CARL JOHAN AURELL , JOHN FRITIOF PONTEN , KEVIN JAMES DOYLE , AMANDA JANE VAN DE POEL , GRAHAM PETER JONES , DAVID WYN WATSON , JAQUELINE ANNE MACRITCHIE , NICHOLAS JOHN PALMER
发明人： HANS ROLAND LONN , STEPHEN CONNOLLY , STEVEN SWALLOW , STAFFAN PO KARLSSON , CARL JOHAN AURELL , JOHN FRITIOF PONTEN , KEVIN JAMES DOYLE , AMANDA JANE VAN DE POEL , GRAHAM PETER JONES , DAVID WYN WATSON , JAQUELINE ANNE MACRITCHIE , NICHOLAS JOHN PALMER
摘要： The present disclosure relates to certain (2S)-N-[(1S)-1-cyano-2-phenylethyl]-1,4-oxazepane-2-carboxamide compounds (including pharmaceutically acceptable salts thereof),that inhibit dipeptidyl peptidase 1 (DPP1) activity, to their utility in treating and/or preventing clinical conditions including respiratory diseases, such as asthma and chronic obstructive pulmonary disease (COPD), to their use in therapy, to pharmaceutical compositions containing them and to processes for preparing such compounds.

2. 发明专利

IL265611D0 (2s)-n-[(1s)-1-cyano-2-phenylethyl]-1,4-oxazepane-2-carboxamides as dipeptidyl peptidase i inhibitors 未知
公开(公告)号：IL265611D0
公开(公告)日：2019-05-30
申请号：IL26561119
申请日：2019-03-25
申请人： ASTRAZENECA AB , HANS ROLAND LONN , STEPHEN CONNOLLY , STEVEN SWALLOW , STAFFAN PO KARLSSON , CARL JOHAN AURELL , JOHN FRITIOF PONTEN , KEVIN JAMES DOYLE , AMANDA JANE VAN DE POEL , GRAHAM PETER JONES , DAVID WYN WATSON , JAQUELINE ANNE MACRITCHIE , NICHOLAS JOHN PALMER
发明人： HANS ROLAND LONN , STEPHEN CONNOLLY , STEVEN SWALLOW , STAFFAN PO KARLSSON , CARL-JOHAN AURELL , JOHN FRITIOF PONTEN , KEVIN JAMES DOYLE , AMANDA JANE VAN DE POEL , GRAHAM PETER JONES , DAVID WYN WATSON , JAQUELINE ANNE MACRITCHIE , NICHOLAS JOHN PALMER
IPC分类号： C07D20060101
摘要： The present disclosure relates to certain (2S)-N-[(1S)-1-cyano-2-phenylethyl]-1,4-oxazepane-2-carboxamide compounds (including pharmaceutically acceptable salts thereof),that inhibit dipeptidyl peptidase 1 (DPP1) activity, to their utility in treating and/or preventing clinical conditions including respiratory diseases, such as asthma and chronic obstructive pulmonary disease (COPD), to their use in therapy, to pharmaceutical compositions containing them and to processes for preparing such compounds.

3. 发明专利

AU3977400A Fishing rod holder 未知
公开(公告)号：AU3977400A
公开(公告)日：2000-10-23
申请号：AU3977400
申请日：2000-04-05
申请人： NICHOLAS JOHN PALMER
发明人： PALMER NICHOLAS JOHN
IPC分类号： A01K97/10 , A01K97/00

4. 发明申请

US20130217664A1 NOVEL COMPOUNDS USEFUL FOR THE TREATMENT OF DEGENERATIVE AND INFLAMMATORY DISEASES 审中-公开
标题翻译：用于治疗衰老和炎症疾病的新型化合物
公开(公告)号：US20130217664A1
公开(公告)日：2013-08-22
申请号：US13762155
申请日：2013-02-07
申请人： Christel Jeanne Marie MENET , Benoit Antoine SCHMITT , Raphael Jean Joel GENEY , Kevin James DOYLE , Joanne PEACH , Nicholas John PALMER , Graham Peter JONES , David HARDY , James Edward Stewart DUFFY
发明人： Christel Jeanne Marie MENET , Benoit Antoine SCHMITT , Raphael Jean Joel GENEY , Kevin James DOYLE , Joanne PEACH , Nicholas John PALMER , Graham Peter JONES , David HARDY , James Edward Stewart DUFFY
IPC分类号： C07D471/04 , A61K31/506 , A61K31/496 , A61K31/541 , A61K31/4545 , A61K31/5377 , A61K31/497 , A61K45/06 , A61K31/444 , A61K31/437 , C07D491/107
CPC分类号： C07D471/04 , A61K31/437 , A61K31/444 , A61K31/4545 , A61K31/496 , A61K31/497 , A61K31/506 , A61K31/5377 , A61K31/541 , A61K45/06 , C07D403/12 , C07D491/107
摘要： Novel imidazolopyridines according to Formula I, able to inhibit JAK are disclosed, these compounds may be prepared as a pharmaceutical composition, and may be used for the prevention and treatment of a variety of conditions in mammals including humans, including by way of non-limiting example, allergic or inflammatory conditions, autoimmune diseases, proliferative diseases, transplantation rejection, diseases involving impairment of cartilage turnover, congenital cartilage malformations, and/or diseases associated with hypersecretion of IL6 or interferons. Wherein R1, L1, R3, R4, Cy, L2 and R5 are as defined herein.
摘要翻译：公开了能够抑制JAK的式I的新型咪唑并吡啶，这些化合物可以制备成药物组合物，并且可以用于预防和治疗包括人在内的哺乳动物中的各种病症，包括通过非限制性的方式例如过敏或炎症状况，自身免疫性疾病，增殖性疾病，移植排斥反应，涉及软骨周转损害的疾病，先天性软骨畸形和/或与IL6或干扰素分泌过多相关的疾病。其中R1，L1，R3，R4，Cy，L2和R5如本文所定义。

5. 发明授权

US08481544B2 Antibacterial compositions 有权
标题翻译：抗菌组合物
公开(公告)号：US08481544B2
公开(公告)日：2013-07-09
申请号：US13154485
申请日：2011-06-07
申请人： David John Haydon , Lloyd George Czaplewski , Nicholas John Palmer , Dale Robert Mitchell , John Frederick Atherall , Christopher Richard Steele , Tamara Ladduwahetty
发明人： David John Haydon , Lloyd George Czaplewski , Nicholas John Palmer , Dale Robert Mitchell , John Frederick Atherall , Christopher Richard Steele , Tamara Ladduwahetty
IPC分类号： A61K31/497 , A61K31/4365 , C07D241/12 , C07D513/04
CPC分类号： A61K31/437 , A01N47/36 , A61K31/4375 , A61K31/4439 , A61K31/444 , A61K31/496 , A61K31/497 , A61K31/501 , A61K31/506 , A61K31/5377 , A61K31/5383
摘要： Compounds of formula (I) have antibacterial activity: wherein: m is 0 or 1; Q is hydrogen or cyclopropyl; Alk is an optionally substituted, divalent C1-C6 alkylene, alkenylene or alkynylene radical which may contain an ether (—O—), thioether (—S—) or amino (—NR)— link, wherein R is hydrogen, —CN or C1-C3 alkyl; X is —C(═O)NR6—, —S(O)NR6—, —C(═O)O— or —S(═O)O— wherein R6 is hydrogen, optionally substituted C1-C6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl, -Cyc, or —(C1-C3 alkyl)-Cyc wherein Cyc is optionally substituted monocyclic carbocyclic or heterocyclic having 3-7 ring atoms; Z is N; R2 and R3 are as defined in the description.
摘要翻译：式（I）化合物具有抗菌活性：其中：m为0或1; Q是氢或环丙基; Alk是可以含有醚（-O-），硫醚（-S-）或氨基（-NR） - 连接的任意取代的二价C1-C6亚烷基，亚烯基或亚炔基，其中R是氢，-CN或 C1-C3烷基; X是-C（= O）NR 6 - ， - S（O）NR 6 - ， - C（= O）O-或-S（= O）O-，其中R 6是氢，任选取代的C 1 -C 6烷基， C6链烯基，C2-C6炔基，-Cyc或 - （C1-C3烷基）-Cyc，其中Cyc是具有3-7个环原子的任选取代的单环碳环或杂环; Z是N; R2和R3如说明书中所定义。

6. 发明授权

US08193215B2 Thieno[2 3-b]pyridines as potassium channel inhibitors 有权
标题翻译：噻吩并[2,3-b]吡啶作为钾通道抑制剂
公开(公告)号：US08193215B2
公开(公告)日：2012-06-05
申请号：US12543151
申请日：2009-08-18
申请人： John Ford , Nicholas John Palmer , John Frederick Atherall , David John Madge , Derek John
发明人： John Ford , Nicholas John Palmer , John Frederick Atherall , David John Madge , Derek John
IPC分类号： A01N43/42
CPC分类号： C07D495/04 , C07D333/36 , C07D333/38 , C07D409/12
摘要： The invention provides compounds of the formula: wherein R1 is aryl, heteroaryl, cycloalkyl or alkyl; R2 is H, alkyl, nitro, CO2R7, CONR5R6 or halo; R3 and R4 are H, NR5R6, NC(O)R7, halo, trifluromethyl, alkyl, CONR5R6, CO2R7, nitrile or alkoxy; R5 and R6 may be the same or different and may be H, alkyl, aryl, heteroaryl or cycloalkyl; or R5 and R6 may together form a saturated, unsaturated or partially saturated 4 to 7 member ring, wherein said ring may optionally comprise one or more further heteroatoms selected from N, O or S; R7 is H or alkyl; A is H, halo, or a group of formula X-L-Y; X is O, S or NR8; R8 is H or alkyl; L is (CH2)n, where n is 0, 1, 2, 3 or 4; and Y is aryl, a heterocyclic group, alkyl, alkenyl or cycloalkyl; the products of mono- and di-oxidation of sulphur and/or mono-oxidation of nitrogen moieties in compounds of formula I; or a pharmaceutically acceptable salt thereof. These compounds find use as inhibitors of potassium ion channels and thus are useful in the treatment of various conditions including arrhythmia and type-2 diabetes mellitus.
摘要翻译：本发明提供下式的化合物：其中R1是芳基，杂芳基，环烷基或烷基; R2是H，烷基，硝基，CO 2 R 7，CONR 5 R 6或卤素; R3和R4是H，NR5R6，NC（O）R7，卤素，三氟甲基，烷基，CONR5R6，CO2R7，腈或烷氧基; R5和R6可以相同或不同，可以是H，烷基，芳基，杂芳基或环烷基; 或R 5和R 6可以一起形成饱和的，不饱和的或部分饱和的4至7元环，其中所述环可任选地包含一个或多个选自N，O或S的其它杂原子; R7是H或烷基; A是H，卤素或式X-L-Y基团; X是O，S或NR8; R8是H或烷基; L是（CH 2）n，其中n是0,1,2,3或4; Y为芳基，杂环基，烷基，链烯基或环烷基; 式I化合物中硫的单和二氧化和/或氮部分的单氧化的产物; 或其药学上可接受的盐。这些化合物可用作钾离子通道的抑制剂，因此可用于治疗各种病症，包括心律失常和2型糖尿病。

7. 发明申请

US20110263590A1 Antibacterial Compositions 有权
标题翻译：抗菌组合物
公开(公告)号：US20110263590A1
公开(公告)日：2011-10-27
申请号：US13154592
申请日：2011-06-07
申请人： David John Haydon , Lloyd George Czaplewski , Nicholas John Palmer , Dale Robert Mitchell , John Frederick Atherall , Christopher Richard Steele , Tamara Ladduwahetty
发明人： David John Haydon , Lloyd George Czaplewski , Nicholas John Palmer , Dale Robert Mitchell , John Frederick Atherall , Christopher Richard Steele , Tamara Ladduwahetty
IPC分类号： A61K31/4439 , A61K31/428 , A61K31/497 , A61K31/496 , A61P31/04 , A61K31/506 , A61K31/501 , A61K31/5383 , A61K31/519 , A61K31/444 , A61K31/5377
CPC分类号： C07D417/04 , C07D417/14 , Y02P20/582
摘要： Compounds of formula (I) have antibacterial activity: wherein: m is 0 or 1; Q is hydrogen or cyclopropyl; Alk is an optionally substituted, divalent C1-C6 alkylene, alkenylene or alkynylene radical which may contain an ether (—O—), thioether (—S—) or amino (—NR)— link, wherein R is hydrogen, —CN or C1-C3 alkyl; X is —C(═O)NR6—, —S(O)NR6—, —C(═O)O— or —S(═O)O— wherein R6 is hydrogen, optionally substituted C1-C6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl, -Cyc, or —(C1-C3 alkyl)-Cyc wherein Cyc is optionally substituted monocyclic carbocyclic or heterocyclic having 3-7 ring atoms; Z is N or CH, or CF; R2 and R3 are as defined in the description.
摘要翻译：式（I）化合物具有抗菌活性：其中：m为0或1; Q是氢或环丙基; Alk是可以含有醚（-O-），硫醚（-S-）或氨基（-NR） - 连接的任意取代的二价C1-C6亚烷基，亚烯基或亚炔基，其中R是氢，-CN或 C1-C3烷基; X是-C（= O）NR 6 - ， - S（O）NR 6 - ， - C（= O）O-或-S（= O）O-，其中R 6是氢，任选取代的C 1 -C 6烷基， C6链烯基，C2-C6炔基，-Cyc或 - （C1-C3烷基）-Cyc，其中Cyc是具有3-7个环原子的任选取代的单环碳环或杂环; Z是N或CH，或CF; R2和R3如说明书中所定义。

8. 发明授权

US08022076B2 Substituted thieno[2,3-d]pyrimidines as potassium channel inhibitors 有权
标题翻译：取代噻吩并[2,3-d]嘧啶作为钾通道抑制剂
公开(公告)号：US08022076B2
公开(公告)日：2011-09-20
申请号：US10864771
申请日：2004-06-10
申请人： John Ford , Nicholas John Palmer , John Frederick Atherall , David John Madge , Brad Sherborne , Mark Bushfield , Edward Benedict Stevens
发明人： John Ford , Nicholas John Palmer , John Frederick Atherall , David John Madge , Brad Sherborne , Mark Bushfield , Edward Benedict Stevens
IPC分类号： C07D495/04 , A61K31/519 , A61P9/06
CPC分类号： A61K31/495 , C07D495/04
摘要： This invention relates to novel compound of formula (I) or pharmaceutically acceptable salts thereof. The invention is also directed to the uses of compounds having formula (I) in the treatment or prevention of diseases or disorders which requires potassium channel inhibition to an animal, mammal or human in need thereof. The invention is also directed to the use of compounds having formula (I) in the treatment or prevention of arrhythmia to an animal, mammal or human in need thereof.
摘要翻译：本发明涉及新的式（I）化合物或其药学上可接受的盐。本发明还涉及具有式（I）的化合物在治疗或预防需要钾通道抑制的疾病或病症中对于有需要的动物，哺乳动物或人的用途。本发明还涉及具有式（I）的化合物在治疗或预防心律失常的用途对于有需要的动物，哺乳动物或人类的用途。

9. 发明申请

US20110166147A1 IMIDAZOPYRAZINE COMPOUNDS 失效
标题翻译：咪唑并吡嗪化合物
公开(公告)号：US20110166147A1
公开(公告)日：2011-07-07
申请号：US12674525
申请日：2008-08-20
申请人： Angus Macleod , Dale Robert Mitchell , Nicholas John Palmer , Michael Daniel Goldsmith , Clifford John Harris , Christophe Claude Parsy
发明人： Angus Macleod , Dale Robert Mitchell , Nicholas John Palmer , Michael Daniel Goldsmith , Clifford John Harris , Christophe Claude Parsy
IPC分类号： C07D487/04 , A61K31/4985 , A61K31/5377 , A61P31/12
CPC分类号： C07D487/04
摘要： Novel imidazopyrazine compounds are disclosed that have a formula represented by the following: Formula (I). The compounds may be prepared as pharmaceutical compositions, and may be used for the prevention and treatment of a viral infection, in particular a HCV, HRV, Sb and/or CVB in a patient in need thereof.
摘要翻译：公开了具有由下式表示的式的新型咪唑并吡嗪化合物：式（I）。化合物可以制备成药物组合物，并且可用于预防和治疗有需要的患者中的病毒感染，特别是HCV，HRV，Sb和/或CVB。

10. 发明申请

US20090197877A1 Antibacterial Compositions 有权
标题翻译：抗菌组合物
公开(公告)号：US20090197877A1
公开(公告)日：2009-08-06
申请号：US12304303
申请日：2007-06-21
申请人： David John Haydon , Lloyd George Czaplewski , Nicholas John Palmer , Dale Robert Mitchell , John Frederick Atherall , Christopher Richard Steele , Tamara Ladduwahetty
发明人： David John Haydon , Lloyd George Czaplewski , Nicholas John Palmer , Dale Robert Mitchell , John Frederick Atherall , Christopher Richard Steele , Tamara Ladduwahetty
IPC分类号： A61K31/5383 , C07D417/10 , A61K31/4439 , A61K31/496 , C07D417/14 , C07D498/04 , A61P31/04
CPC分类号： C07D417/04 , C07D417/14 , Y02P20/582
摘要： Compounds of formula (I) have antibacterial activity: wherein: m is 0 or 1; Q is hydrogen or cyclopropyl; AIk is an optionally substituted, divalent C1-C6 alkylene, alkenylene or alkynylene radical which may contain an ether (—O—), thioether (—S—) or amino (—NR)— link, wherein R is hydrogen, —CN or C1-C3 alkyl; X is —C(═O)NR6—, —S(O)NR6—, —C(═O)O— or —S(═O)O— wherein R6 is hydrogen, optionally substituted C1-C6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl, -Cyc, or —(C1-C3 alkyl)-Cyc wherein Cyc is optionally substituted monocyclic carbocyclic or heterocyclic having 3-7 ring atoms; Z is N or CH, or CF; R2 and R3 are as defined in the description.
摘要翻译：式（I）化合物具有抗菌活性：其中：m为0或1; Q是氢或环丙基; Alk是可以含有醚（-O-），硫醚（-S-）或氨基（-NR） - 连接的任意取代的二价C 1 -C 6亚烷基，亚烯基或亚炔基，其中R是氢，-CN或 C1-C3烷基; X是-C（-O）NR 6 - ， - S（O）NR 6 - ， - C（-O）O-或-S（-O）O-，其中R 6是氢，任选取代的C 1 -C 6烷基， C6链烯基，C2-C6炔基，-Cyc或 - （C1-C3烷基）-Cyc，其中Cyc是具有3-7个环原子的任选取代的单环碳环或杂环; Z是N或CH，或CF; R2和R3如说明书中所定义。

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