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1. 发明公开

KR1020000049048A 인터루킨-1β 전환 효소의 아스파르테이트 에스테르 억제제 无效
标题翻译：白介素-1转化酶的ASPARTATE ESTER抑制剂
公开(公告)号：KR1020000049048A
公开(公告)日：2000-07-25
申请号：KR1019997003117
申请日：1997-10-09
申请人： 워너-램버트 캄파니 엘엘씨 , 바스프 에스이
发明人： 알브레히트,한스,페. , 알렌,해미쉬,존 , 브래디,케니쓰,데일 , 캐프레이드,브래들리,윌리암 , 길모어,존,로쥐 , 하터,윌리암,글렌 , 헤이스,쉐릴,진 , 코스틀란,캐서린,로즈 , 루니,엘리자베쓰,앤 , 파라,킴벌리,수잔 , 토마스,앤쏘니,제롬 , 워커,니겔
IPC分类号： C07C271/22
CPC分类号： C07D207/08 , A61K38/00 , C07C233/47 , C07C233/51 , C07C271/22 , C07C275/16 , C07C311/03 , C07C311/06 , C07C311/19 , C07C317/04 , C07C317/44 , C07C323/52 , C07C327/32 , C07C2601/10 , C07C2602/10 , C07C2602/42 , C07D207/27 , C07D207/28 , C07D209/08 , C07D209/18 , C07D211/34 , C07D211/76 , C07D213/55 , C07D213/75 , C07D217/24 , C07D233/36 , C07D239/10 , C07D307/79 , C07D333/24 , C07D333/38 , C07D333/54 , C07K5/0202
摘要： PURPOSE: Provided are compounds which are inhibitors of interleukin-1ss converting enzyme. Also a method of treatment of stroke, reperfusion injury, Alzheimer's disease, shigellosis, inflammatory diseases, and a pharmaceutically acceptable composition containing the compound are provided. CONSTITUTION: Compounds which are inhibitors of interleukin-1 beta converting enzyme that have formula (I) wherein R¬1 is R¬3CO-, R¬3SO2-, each R¬a is independently hydrogen, C1-C6 alkyl, or -(CH2)n aryl; R¬2 is -(CRR)n-aryl, -(CRR)n-X-aryl, -(CRR)n-heteroaryl, -(CRR)n-X-heteroaryl, -(CRR)n-(substituted-heteroaryl), -(CRR)n-(substituted-aryl), -(CRR)n-X-(substituted-aryl), -(CRR)n-aryl-aryl, -(CRR)n-aryl-heteroaryl, -(CRR)n-aryl-(CH2)n-aryl, -(CRR)n-CH(aryl)2, -(CRR)n-cycloalkyl, -(CRR)n-X-cycloalkyl, -(CRR)n-heterocycle, -(CRR)n-X-heterocycle, -(CRR)n substituted heterocycle, each R is independently hydrogen, C1-C6 alkyl, halogen or hydroxy; X is O or S; R3 is C1 -C6 alkyl, aryl heteroaryl, -(CHR)n-aryl, -(CHR)n-heteroaryl, -(CHR)n-substituted heteroaryl, -(CHR)n-substituted aryl, -(CRR)nS(CH2)n-aryl, cycloalkyl, substituted cycloalkyl, heterocycle, substituted heterocycle, each R¬1 is independently C1-C6 alkyl, C1 -C6 alkylaryl, aryl, or hydrogen; each J is independently -C02R¬b, -CONR¬bR¬b, -SO2NR¬bR¬b, or -SO2R¬b; each R¬b is independently hydrogen, C1-C6 alkyl, aryl, substituted aryl; arylalkyl, heteroarylalkyl, substituted arylalkyl, or substituted heteroarylalkyl; R4 is hydrogen, C1-C6 alkyl, -phenyl, R6 is hydrogen, C 1 -C6 alkyl, -(CH2)n aryl, -(CH2)nCO2Ra, hydroxyl substituted C1-C6 alkyl, or imidazole substituted C1-C6 alkyl; each n is independently 0 to 3, and the pharmaceutically acceptable, salts, esters, amides, and prodrugs thereof.
摘要翻译：目的：提供作为白细胞介素-1β转换酶抑制剂的化合物。还提供了治疗中风，再灌注损伤，阿尔茨海默病，志贺氏菌病，炎性疾病和含有该化合物的药学上可接受的组合物的方法。构成：具有式（I）的式I化合物的化合物，其中R 1是R 3 CO-，R 3 SO 2 - ，各R aa独立地是氢，C 1 -C 6烷基或 - （ CH2）n芳基; R 2是 - （CRR）n - 芳基， - （CRR）n -X-芳基， - （CRR）n - 杂芳基 - （CRR）n X - 杂芳基 - （CRR）n-（取代杂芳基） CRR）n-（取代的 - 芳基）， - （CRR）nX-（取代的 - 芳基）， - （CRR）n-芳基 - - （CRR）n-芳基杂芳基， - （CRR）（CRR）n - 芳基， - （CRR）n-CH（芳基）2， - （CRR）n - 环烷基， - （CRR）， - （CRR）n取代的杂环，每个R独立地是氢，C 1 -C 6烷基，卤素或羟基; X是O或S; R 3是C 1 -C 6烷基，芳基杂芳基， - （CHR）n - 芳基， - （CHR）n - 杂芳基 - （CHR）n - 取代杂芳基， - （CHR）n-取代芳基 - （CRR） CH 2）n - 芳基，环烷基，取代的环烷基，杂环，取代的杂环，各R 1独立地是C 1 -C 6烷基，C 1 -C 6烷基芳基，芳基或氢; 每个J独立地为-CO 2 R b，-CONR b R b，-SO 2 NR a b R b b或-SO 2 R bb; 每个R b独立地是氢，C 1 -C 6烷基，芳基，取代的芳基; 芳基烷基，杂芳基烷基，取代的芳基烷基或取代的杂芳基烷基; R 4是氢，C 1 -C 6烷基， - 苯基，R 6是氢，C 1 -C 6烷基， - （CH 2）n芳基， - （CH 2）n CO 2 R a，羟基取代的C 1 -C 6烷基或咪唑取代的C 1 -C 6烷基; 每个n独立地为0至3，以及其药学上可接受的盐，酯，酰胺和前药。

2. 发明公开

KR1020000049050A 술폰아미드 치환된 아스파르트산 인터루킨-1β 전환 효소 억제제 无效
标题翻译：磺酰胺取代的ASPACTIC ACID INTERLEUKIN-1 BETA转换酶抑制剂
公开(公告)号：KR1020000049050A
公开(公告)日：2000-07-25
申请号：KR1019997003119
申请日：1997-10-09
申请人： 워너-램버트 캄파니 엘엘씨 , 바스프 에스이
发明人： 알렌,해미쉬,존 , 브래디,케니쓰,데일 , 하터,윌리암,글렌 , 루니,엘리자베쓰,앤 , 플러머,마크,스티븐 , 소워,토미 , 샤리푸어,오래쉬 , 워커,니겔
IPC分类号： C07C311/29
CPC分类号： C07D307/12 , C07C311/19 , C07C311/29 , C07C311/46 , C07C323/67 , C07C2601/14 , C07C2602/10
摘要： PURPOSE: Provided are compounds which are inhibitors of interleukin- I p converting enzyme. Also provided is a method of treatment of stroke, inflammatory diseases, septic shock, reperfusion injury, Alzheimer's disease, shigellosis, and to a pharmaceutically acceptable composition that contains a compound that is an inhibitor of interleukin-1P converting enzyme. CONSTITUTION: Compounds are illustrated by the Formula I wherein R1 is hydrogen, C1-C6alkyl, or benzyl; R2 is -CHO, -CORa, or -CN; each Ra is independently hydrogen or Cl-C6alkyl; X is a bond, CH2, CHR5, NH, NR5, or O; R3 is aryl, substituted-aryl, heteroaryl, substituted-heteroaryl, cycloalkyl, substituted-cycloalkyl, heterocycle, or substituted-heterocycle; Y is absent, NR5, CO, S, O, SO2, -o(CHR5)n-, CHR5, NR5CO, CONR5, OCHR5, CHR5O, SCHR5, CHR5S, SO2NR5, C1-C6alkyl, NR5SO2, CH2CHR5, CHR5CH2, COCH2, or CH2CO; R4 is absent, aryl, substituted-aryl, Cl-Cgalkyl, heteroaryl, substituted-heteroaryl, cycloalkyl, Cl-C6alkyl, substituted-cycloalkyl, heterocycloalkyl, or substituted-heterocycloalkyl; each R5 is independently hydrogen, C1-C6alkyl, aryl, -(CH2)naryl, or -(CH2)ncycloalkyl; each n is independently 0 to 5, m is 1 or 2, and the pharmaceutically acceptable salts, esters, amides, and prodrugs thereof.
摘要翻译：目的：提供作为白细胞介素-I p转换酶抑制剂的化合物。还提供了治疗中风，炎性疾病，败血性休克，再灌注损伤，阿尔茨海默病，志贺氏菌病的方法，以及含有作为白细胞介素-1P转化酶抑制剂的化合物的药学上可接受的组合物。构成：化合物由式I表示，其中R 1是氢，C 1 -C 6烷基或苄基; R2是-CHO，-CORa或-CN; 每个R a独立地是氢或C 1 -C 6烷基; X是键，CH2，CHR5，NH，NR5或O; R 3为芳基，取代芳基，杂芳基，取代杂芳基，环烷基，取代环烷基，杂环或取代杂环; Y不存在，NR 5，CO，S，O，SO 2，-o（CHR 5）n - ，CHR 5，NR 5 CO，CONR 5，OCHR 5，CHR 5 O，SCHR 5，CHR 5 S，SO 2 NR 5，C 1 -C 6烷基，NR 5 SO 2，CH 2 CHR 5，CHR 5 CH 2，COCH 2，或CH 2 CO; R 4不存在，芳基，取代的芳基，C 1 -C 8烷基，杂芳基，取代的杂芳基，环烷基，C 1 -C 6烷基，取代的环烷基，杂环烷基或取代的 - 杂环烷基; 每个R 5独立地是氢，C 1 -C 6烷基，芳基， - （CH 2）n芳基或 - （CH 2）n环烷基; 每个n独立地为0至5，m为1或2，以及其药学上可接受的盐，酯，酰胺和前药。

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