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1. 发明公开

EP0528633A1 Pyrimidinyl acetamides as elastase inhibitors 失效
标题翻译：嘧啶基 - Essigsäureamideals弹性蛋白酶抑制剂。
公开(公告)号：EP0528633A1
公开(公告)日：1993-02-24
申请号：EP92307389.4
申请日：1992-08-12
申请人： ZENECA LIMITED
发明人： Bernstein, Peter Robert , Edwards, Philip Duke , Shaw, Andrew , Thomas, Royston Martin , Veale, Chris Allan , Warner, Peter , Wolanin, Donald John
IPC分类号： C07D239/46 , C07D401/04 , C07D401/12 , C07D409/04 , A61K31/505
CPC分类号： C07D239/47 , A61K38/00 , C07D401/04 , C07D401/12 , C07D401/14 , C07D409/04 , C07D409/14 , C07K5/06191
摘要： The present invention relates to certain nobel substituted heterocycles which are 1-pyrimidinylacetamide compounds of formula I, set out herein, which are inhibitors of human leukocyte elastase (HLE), also known as human neutrophil elastase (HNE), making them useful whenever such inhibition is desired, such as for research tools in pharmacological, diagnostic and related studies and in the treatment of diseases in mammals in which HLE is implicated. The invention also includes intermediates useful in the synthesis of these substituted heterocycles, processes for preparing the substituted heterocycles, pharmaceutical compositions containing such substituted heterocycles and methods for their use.
摘要翻译：本发明涉及作为人类白细胞弹性蛋白酶（HLE）抑制剂（也称为人嗜中性粒细胞弹性蛋白酶（HNE））的本文列出的作为式I的1-嘧啶基乙酰胺化合物的某些诺贝尔取代的杂环，使得它们在这种抑制是期望的，例如在药理学，诊断学和相关研究中的研究工具以及涉及HLE的哺乳动物疾病的治疗。本发明还包括可用于合成这些取代的杂环的中间体，制备取代的杂环的方法，含有这种取代杂环的药物组合物及其使用方法。

2. 发明公开

EP0509769A3 Heterocyclic amides having HLE inhibiting activity 失效
标题翻译：具有HLE抑制活性的杂环化合物
公开(公告)号：EP0509769A3
公开(公告)日：1993-09-01
申请号：EP92303358.3
申请日：1992-04-15
申请人： ZENECA LIMITED
发明人： Bernstein, Peter Robert, ICI Americas Inc , Shaw, Andrew, ICI Americas Inc , Thomas, Royston Martin, ICI Americas Inc , Wolanin, Donald John, ICI Americas Inc , Warner, Peter
IPC分类号： C07K5/08 , C07K5/06 , A61K38/55
CPC分类号： C07K5/06191 , A61K38/00
摘要： The present invention relates to certain novel heterocyclic amides which are 1-pyridylacetamide compounds of formula I, set out herein, which are inhibitors of human leukocyte elastase (HLE), also known as human neutrophil elastase (HNE), making them useful whenever such inhibition is desired, such as for research tools in pharmacological, diagnostic and related studies and in the treatment of diseases in mammals in which HLE is implicated. The invention also includes intermediates useful in the synthesis of these heterocyclic amides, processes for preparing the heterocyclic amides, pharmaceutical compositions containing such heterocyclic amides and methods for their use.

3. 发明授权

EP0528633B1 Pyrimidinyl acetamides as elastase inhibitors 失效
标题翻译：嘧啶基Essigsäureamide如弹性蛋白酶抑制剂
公开(公告)号：EP0528633B1
公开(公告)日：2000-10-18
申请号：EP92307389.4
申请日：1992-08-12
申请人： ZENECA LIMITED
发明人： Bernstein, Peter Robert , Edwards, Philip Duke , Shaw, Andrew , Thomas, Royston Martin , Veale, Chris Allan , Warner, Peter , Wolanin, Donald John
IPC分类号： C07D239/46 , C07D401/04 , C07D401/12 , C07D409/04 , A61K31/505
CPC分类号： C07D239/47 , A61K38/00 , C07D401/04 , C07D401/12 , C07D401/14 , C07D409/04 , C07D409/14 , C07K5/06191

4. 发明公开

EP0752421A1 Ortho-substituted aromatic compounds, containing three (het)aryl moieties, their preparation and their use as prostaglandin E2-(PGE2)-antagonists 失效
标题翻译：邻位取代的含有3（杂）芳基环，它们的制备以及它们作为前列腺素E2（PGE2）拮抗剂的用途的芳族化合物
公开(公告)号：EP0752421A1
公开(公告)日：1997-01-08
申请号：EP96304888.9
申请日：1996-07-02
申请人： ZENECA LIMITED
发明人： Breault, Gloria Anne , Oldfield, John , Tucker, Howard , Warner, Peter
IPC分类号： C07D213/40 , C07D213/55 , C07D213/74 , C07D213/75 , A61K31/44 , C07D233/54 , A61K31/415 , C07D237/24 , A61K31/50 , C07C63/04 , C07C63/64 , A61K31/19 , C07C65/05 , C07C65/21 , C07C229/38 , C07C229/52 , C07C229/60 , C07C233/65 , C07C233/69 , C07C237/30 , C07C237/32 , C07C323/32 , C07C323/62
CPC分类号： C07D213/75 , C07C63/331 , C07C65/105 , C07C65/24 , C07C229/38 , C07C229/52 , C07C229/60 , C07C233/65 , C07C233/69 , C07C237/30 , C07C237/32 , C07C323/62 , C07D213/55 , C07D213/80 , C07D233/64 , C07D237/24
摘要： The invention relates to compounds of the formula
wherein:

A is an optionally substituted ring system provided that the -Z-B-R 1 and -X-D linking groups are positioned in a 1,2 relationship to one another on ring carbon atoms and the ring atom positioned ortho to the -X- linking group (and therefore in the 3-position relative to the -Z- linking group) is not substituted;
B is an optionally substituted ring system
D is optionally substituted: pyridyl, pyrazinyl, pyrimidinyl, pyridazinyl, pyrrolyl, thienyl, furyl, imidazolyl, pyrazolyl, thiazolyl, isothiazolyl, oxazolyl, isoxazolyl or phenyl;
R 1 is positioned on ring B in a 1,3 or 1,4 relationship with the -Z- linking group in 6-membered rings and in a 1,3-relationship with the -Z- linking group in 5-membered rings and is as defined in the description;
X is -OCH 2- , -SCH 2- , -CH 2 CH 2- , CH 2- , -O-, -S- or -N(R 4 )CH 2- wherein the left hand atom is attached to A and the right hand atom is attached to D;
Z is of the formula -CH(R 3 )CH(R 3 )N(R 2 )-, -N(R 2 )CH(R 3 )-, -CH(R 3 )P 1 -, -(CH(R 3 ))m- or -CH(R 3 )N(R 2 )-
wherein
R 2 is hydrogen, C 1-6 alkyl (optionally substituted by hydroxy, cyano, nitro, amino, halo, C 1-4 alkanoyl, C 1-4 alkoxy or trifluoromethyl) C 2-6 alkenyl, C 2-6 alkynyl, C 3-6 cycloalkyl, C 3-6 cycloalkylC 1-3 alkyl, C 3-6 cycloalkylC 2-3 alkenyl, C 5-6 cycloalkenyl, C 5-6 cycloalkenylC 1-3 alkyl, C 5-6 cycloalkenylC 2-3 alkenyl, phenyl, phenylC 1-3 alkyl or 5- or 6-membered heteroarylC 1-3 alkyl;
R 3 is hydrogen or C 1-4 alkyl;
P 1 is oxygen or sulphur, m is 2 or 3 and R 4 is hydrogen or C 1-4 alkyl and wherein the left hand atom is attached to A and the right hand atom is attached to B; provided that when Z is -CH(R 3 )N(R 2 )- or -(CH(R 3 ))m-, X is not -OCH 2 -; and N-oxides of -NR 2 where chemically possible;
and S-oxides of sulphur containing rings where chemically possible;
and pharmaceutically acceptable salts and in vivo hydrolysable esters and amides thereof.

Processes for their preparation, intermediates in their preparation, their use as pharmaceutical agents and pharmaceutical compositions containing them.
The compounds of the invention are useful in the treatment of pain such as the pain associated with joint conditions (such as rheumatoid arthritis and osteoarthritis), postoperative pain, post-partum pain, the pain associated with dental conditions (such as dental caries and gingivitis), the pain associated with burns (including sunburn), the treatment of bone disorders (such as osteoporosis, hypercalcaemia of malignancy and Paget's disease), the pain associated with sports injuries and sprains and all other painful conditions in which E-type prostaglandins wholly or in part play a pathophysiological role.
摘要翻译：本发明涉及下式的化合物 worin：A是任选substituiertem环系统提供DASS死-ZBR <1>和-Xd连接基团在1,2关系彼此在环碳原子和被定位环原子邻位的-X-的连接基团（并且相对于-Z-连接基团的3位在THEREFORE）不substituiertem; B是任选substituiertem环系统D是任选substituiertem：吡啶基，吡嗪基，嘧啶基，哒嗪基，吡咯基，噻吩基，呋喃基，咪唑基，吡唑基，噻唑基，异噻唑基，恶唑基，异恶唑基或苯基; [R <1>与-Z-连接基团1,3-或1,4-关系在5元被定位在环B在6元环，而在与所述-Z-连接基团1,3-关系环和是如说明书中所定义; X是-OCH 2，-SCH 2，-CH 2 CH 2，CH 2，-O - ， - S-或-N（R <4>）CH2 worin左手原子连接于A和右手原子是附着到D; Z为式CH（R <3>）CH（R <3>）N（R <2>） - ， - N（R <2>）CH（R <3>） - ， - CH（R <3>）P <1> - ， - （CH（R <3>））m-或-CH（R <3>）N（R <2>） - 氢worinř<2>是，C 1-6烷基（任选地被羟基，氰基，硝基，氨基，卤素，C1-4alkanoyl，C 1-4烷氧基或三氟甲基substituiertem）C 2-6烯基，C 2-6炔基，C 3-6环烷基，C3-6cycloalkylC1-3alkyl，C3-6cycloalkylC2-3alkenyl，C5- 6cycloalkenyl，C5-6cycloalkenylC1-3alkyl，C5-6cycloalkenylC2-3alkenyl，苯基，phenylC1-3alkyl或5-或6-元heteroarylC1-3alkyl; [R <3>是氢或C 1-4烷基; P <1>为氧或硫，m是2或3，R <4>是氢或C 1-4烷基和worin左手原子连接于A和右手原子连接到B; 提供确实当Z是-CH（R <3>）N（R <2>） - 或 - （CH（R <3>））间 - 时，X不是-OCH 2; 和-NR <2>的N-氧化物在化学上可能; 和含硫环的S-氧化物在化学上可能; 和药学上可接受的盐和体内可水解的酯和酰胺。它们的制备方法，其制备中间体，其作为药物和含有它们的药物组合物。本发明的化合物可用于治疗疼痛的有用：如与关节条件（颜色：如类风湿性关节炎和骨关节炎）相关的疼痛，手术后疼痛，产后疼痛，与牙齿条件（颜色相关的疼痛：如龋齿和牙龈炎），烧伤（包括晒伤相关的疼痛），骨疾病（治疗：如骨质疏松症，恶性高血钙和Paget氏病），与运动损伤和扭伤和其中E型前列腺素全所有其它疼痛病症相关的疼痛或部分发挥病理生理作用。

5. 发明授权

EP0509769B1 Heterocyclic amides having HLE inhibiting activity 失效
标题翻译： HLE抑制剂杂合酰胺
公开(公告)号：EP0509769B1
公开(公告)日：1996-09-11
申请号：EP92303358.3
申请日：1992-04-15
申请人： ZENECA LIMITED
发明人： Bernstein, Peter Robert, ICI Americas Inc , Shaw, Andrew, ICI Americas Inc , Thomas, Royston Martin, ICI Americas Inc , Wolanin, Donald John, ICI Americas Inc , Warner, Peter
IPC分类号： C07K5/08 , C07K5/06 , A61K38/55
CPC分类号： C07K5/06191 , A61K38/00

6. 发明公开

EP0509769A2 Heterocyclic amides having HLE inhibiting activity 失效
标题翻译： HLE抑制剂杂合酰胺。
公开(公告)号：EP0509769A2
公开(公告)日：1992-10-21
申请号：EP92303358.3
申请日：1992-04-15
申请人： ZENECA LIMITED
发明人： Bernstein, Peter Robert, ICI Americas Inc , Shaw, Andrew, ICI Americas Inc , Thomas, Royston Martin, ICI Americas Inc , Wolanin, Donald John, ICI Americas Inc , Warner, Peter
IPC分类号： C07K5/08 , C07K5/06 , A61K38/55
CPC分类号： C07K5/06191 , A61K38/00
摘要： The present invention relates to certain novel heterocyclic amides which are 1-pyridylacetamide compounds of formula I, set out herein, which are inhibitors of human leukocyte elastase (HLE), also known as human neutrophil elastase (HNE), making them useful whenever such inhibition is desired, such as for research tools in pharmacological, diagnostic and related studies and in the treatment of diseases in mammals in which HLE is implicated. The invention also includes intermediates useful in the synthesis of these heterocyclic amides, processes for preparing the heterocyclic amides, pharmaceutical compositions containing such heterocyclic amides and methods for their use.
摘要翻译：本发明涉及某些新颖的杂环酰胺，它们是本文列出的式I的1-吡啶基乙酰胺化合物，其是人类白细胞弹性蛋白酶（HLE）的抑制剂，也被称为人嗜中性粒细胞弹性蛋白酶（HNE）），使得它们在这种抑制是期望的，例如在药理学，诊断学和相关研究中的研究工具以及涉及HLE的哺乳动物疾病的治疗。本发明还包括可用于合成这些杂环酰胺的中间体，制备杂环酰胺的方法，含有这种杂环酰胺的药物组合物及其使用方法。

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