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1. 发明授权

KR100323272B1 치환된 시클릭 아민 메탈로프로테아제 저해제 失效
标题翻译：取代的循环胺金属蛋白酶抑制剂
公开(公告)号：KR100323272B1
公开(公告)日：2002-02-06
申请号：KR1019997001658
申请日：1997-08-22
申请人： 더 프록터 앤드 갬블 캄파니
发明人： 네이쳐스마이클죠지 , 드비즈워나쓰 , 피쿨스태니슬로 , 암스테드네일그레고리 , 북랜드로저군나드 , 타이워예툰데올라비지 , 쳉멘얀
IPC分类号： C07D207/48
CPC分类号： C07D207/42
摘要： 본발명은메탈로프로테아제의억제제로서유용하고, 상기엔자임의과활성으로특정지워지는상태의치료에효과적인화합물을제공한다. 특히, 본발명은화학식 (I)에따른구조를갖는화합물에관한것이다. 또한, 본발명은화합물, 약학조성물및, 상기화합물들, 또는이들을함유한약학조성물을사용한메탈로프로테아제활성으로특정지워지는질병의치료방법을개시한다.

2. 发明公开

KR1020000035925A 매트릭스 메탈로프로테아제 저해제인 포스핀산 아미드 无效
标题翻译：磷酸酰胺作为基质金属蛋白酶抑制剂
公开(公告)号：KR1020000035925A
公开(公告)日：2000-06-26
申请号：KR1019997001661
申请日：1997-08-22
申请人： 더 프록터 앤드 갬블 캄파니
发明人： 피쿨스태니슬로 , 맥도우-던햄켈리린 , 드비즈워나쓰 , 타이워예툰데올라비지
IPC分类号： C07F9/36 , A61K31/66
CPC分类号： C07F9/588 , C07F9/36 , C07F9/587 , C07F9/655345 , Y10S514/824 , Y10S514/861 , Y10S514/863 , Y10S514/864 , Y10S514/886 , Y10S514/902 , Y10S514/903
摘要： PURPOSE: Provided are compounds which are useful as inhibitors of matrix metalloproteases, and which are effective in treating conditions characterized by excess activity of these enzymes. CONSTITUTION: Preferred compounds having a structure according to formula (I) include an optical isomer, a stereoisomer or enantiomer thereof, or a pharmaceutically acceptable salt, or biohydrolyzable alkoxyamide, ester acyloxyamide, imide or derivative thereof. Also provided are compounds, pharmaceutical compositions and methods of treating diseases characterized by matrix metalloprotease activity using these compounds or the pharmaceutical compositions containing them.
摘要翻译：目的：提供可用作基质金属蛋白酶抑制剂的化合物，其有效治疗以这些酶的过量活性为特征的病症。构成：具有式（I）结构的优选化合物包括旋光异构体，立体异构体或其对映异构体，或其药学上可接受的盐或生物可水解的烷氧基酰胺，酯酰氧基酰胺，酰亚胺或其衍生物。还提供了使用这些化合物或含有它们的药物组合物治疗以基质金属蛋白酶活性为特征的疾病的化合物，药物组合物和方法。

3. 发明公开

KR1020000035923A 헤테로고리성 메탈로프로테아제 억제제 失效
标题翻译：金属间化合物的杂环抑制剂
公开(公告)号：KR1020000035923A
公开(公告)日：2000-06-26
申请号：KR1019997001659
申请日：1997-08-22
申请人： 더 프록터 앤드 갬블 캄파니
发明人： 드비즈워나쓰 , 네이쳐스마이클죠지 , 피쿨스태니슬로 , 암스테드네일그레고리 , 매튜랜달스트라이커 , 타이워예툰데올라비지 , 쳉멘얀
IPC分类号： C07D243/08
CPC分类号： C07D265/30 , C07D223/06 , C07D241/04 , C07D241/08 , C07D279/12 , C07D281/00 , C07D281/06 , C07D401/06 , C07D401/12 , C07D405/06 , C07D409/06 , C07D413/06 , C07D417/12 , Y02P20/582
摘要： PURPOSE: Compounds useful for the treatment of conditions and diseases which are characterized by unwanted MP activity and potent inhibitors of metalloproteases are provided. CONSTITUTION: The compounds are those of Formula (I) or a pharmaceutically-acceptable salt, or biohydrolyzable amide, ester, or imide thereof. Pharmaceutically-acceptable carriers or components thereof are sugars, tragacanth, malt, gelatin, talc and etc. In an embodiment of preparation of N-Hydroxy 1N-(4-Methoxyphenyl)sulfonyl-4N-methyl piperazine-2- Carbonari, paraformaldehyde (0.21 g, 6.84 mmol) is added to a solution of methyl ester of 1N-(4-methoxyphenyl)sulfonyl-piperazine-2-carboxyl acid hydrochloride(1.2 g, 3.4 mmol), sodium acetate (0.84 g, 10.26 mmol) in 10 mL of ethanol, followed by sodium cyanoborohydride (0.45 g, 6.84 mmol) slowly at room temperature. The reaction is stirred overnight at room temperature. The reaction mixture is concentrated under reduced pressure and stirred in 1 N HCI for 30 min. The mixture is made basic by 1 N NaOH, and extracted with EtOAc (3 x 80 mL) in the presence of some solid NaCl. The EtOAc layer is washed with brine, dried over MgS04, and concentrated under reduced pressure. The crude product is purified by column chromatography on silica gel using EtOAc.
摘要翻译：目的：提供可用于治疗特征为不需要的MP活性和有效的金属蛋白酶抑制剂的病症和疾病的化合物。构成：化合物为式（I）化合物或其药学上可接受的盐或其可生物水解的酰胺，酯或酰亚胺。药学上可接受的载体或组分是糖，黄蓍胶，麦芽，明胶，滑石等。在制备N-羟基1N-（4-甲氧基苯基）磺酰基-4-甲基哌嗪-2-羰基的实施方案中，将多聚甲醛 g，6.84mmol）加入到1N-（4-甲氧基苯基）磺酰基 - 哌嗪-2-羧酸盐酸盐（1.2g，3.4mmol），乙酸钠（0.84g，10.26mmol）的10ml甲醇溶液的乙醇，然后在室温下缓慢加入氰基硼氢化钠（0.45g，6.84mmol）。将反应物在室温下搅拌过夜。将反应混合物减压浓缩并在1N HCl中搅拌30分钟。混合物通过1N NaOH制成碱性，并在一些固体NaCl存在下用EtOAc（3×80mL）萃取。 EtOAc层用盐水洗涤，用MgSO 4干燥，减压浓缩。粗产物通过硅胶柱色谱纯化，使用EtOAc。

4. 发明公开

KR1020000035918A 1,3-디헤테로시클릭 메탈로프로테아제 저해제 无效
标题翻译： 1,3-二氢化物金属蛋白酶抑制剂
公开(公告)号：KR1020000035918A
公开(公告)日：2000-06-26
申请号：KR1019997001654
申请日：1997-08-22
申请人： 더 프록터 앤드 갬블 캄파니
发明人： 피쿨스태니슬로 , 맥도우-던햄켈리린 , 암스테드네일그레고리 , 드비즈워나쓰 , 네이쳐스마이클죠지 , 타이워예툰데올라비지
IPC分类号： C07D239/04
CPC分类号： C07D239/10 , C07D233/02 , C07D233/38 , C07D239/04 , C07D243/04 , C07D265/06 , C07D265/14 , C07D277/06 , C07D279/06 , C07D409/14 , C07D413/14 , C07D487/04 , C07D495/10
摘要： PURPOSE: Compounds useful for the treatment of conditions and diseases which are characterized by unwanted MP activity, potent inhibitors of metalloproteases, pharmaceutical compositions comprising such inhibitors and a method of treatment for metalloprotease related maladies are provided. CONSTITUTION: The compounds are useful as inhibitors of metalloproteases and effective in treating conditions characterized by excess activity of these enzymes. In particular, the invention relates to a compound having a structure according to Formula (I) wherein R1 is H; R2 is hydrogen, alkyl, or acyl; Ar is COR3 or SO2R4; and R3 is alkoxy, aryloxy, heteroaryloxy, alkyl, aryl, heteroaryl, heteroalkyl, amino, alkylamino, dialkylamino, arylamino and alkylarylamino; R4 is alkyl, heteroalkyl, aryl, or heteroaryl, substituted or unsubstituted; X is O, S, SO, SO2, or NRg, wherein R5 is independently chosen from hydrogen, alkyl, heteroalkyl, heteroaryl, aryl, SO2R6, COR7, CSRg, PO(Rg)2 or may optionally form a ring with Y or W; and R6 is alkyl, aryl, heteroaryl, diarylamino and alkylarylamino; R7 is hydrogen, alkoxy, aryloxy, heteroaryloxy, alkyl, aryl,, dialkylamino, arylamino and alkylarylamino; R8 is alkyl, aryl, heteroaryl, arylamino, diarylamino and alkylarylamino; R9 is alkyl, aryl, heteroaryl, heteroalkyl.
摘要翻译：目的：提供可用于治疗以不需要的MP活性为特征的病症和疾病的化合物，金属蛋白酶的有效抑制剂，包含这些抑制剂的药物组合物和金属蛋白酶相关疾病的治疗方法。构成：这些化合物可用作金属蛋白酶抑制剂，并有效治疗以这些酶的过度活性为特征的病症。特别地，本发明涉及具有式（I）结构的化合物，其中R 1是H; R2是氢，烷基或酰基; Ar为COR3或SO2R4; 芳基，芳基，杂芳基，杂烷基，氨基，烷基氨基，二烷基氨基，芳基氨基和烷芳基氨基; R 4是烷基，杂烷基，芳基或杂芳基，取代或未取代的; X是O，S，SO，SO 2或NR g，其中R5独立地选自氢，烷基，杂烷基，杂芳基，芳基，SO2R6，COR7，CSRg，PO（Rg）2，或者可以任选地形成具有Y或W ; 并且R 6是烷基，芳基，杂芳基，二芳基氨基和烷基芳基氨基; R 7是氢，烷氧基，芳氧基，杂芳氧基，烷基，芳基，二烷基氨基，芳基氨基和烷芳基氨基; R8是烷基，芳基，杂芳基，芳基氨基，二芳基氨基和烷基芳基氨基; R9是烷基，芳基，杂芳基，杂烷基。

5. 发明公开

KR1020000035921A 비덴테이트 메탈로프로테아제 저해제 无效
标题翻译： BIDENTATE METALLOPROTEASE INHIBITORS
公开(公告)号：KR1020000035921A
公开(公告)日：2000-06-26
申请号：KR1019997001657
申请日：1997-08-22
申请人： 더 프록터 앤드 갬블 캄파니
发明人： 암스테드네일그레고리 , 드비즈워나쓰 , 브래들리림마샌들러 , 개럿게리스티븐 , 마를린존에모리2세 , 맥키버존맥밀란 , 왕제 , 타이워예툰데올라비지
IPC分类号： C07D207/48
CPC分类号： C07D401/04 , C07D207/48 , C07D211/96 , C07D401/14 , C07D417/06 , C07D417/14
摘要： PURPOSE: Provided are compositions which are useful for treatment of diseases, disorders or conditions associated with unwanted metalloprotease activity. CONSTITUTION: Provided are compounds which are useful as inhibitors of metalloproteases, and which are effective in treating conditions characterized by excess a metalloprotease activity of decomposing structural proteins. In particular, provided are a compound having a structure according to Formula (I), or an optical isomer, diastereomer or enantiomer thereof, or a pharmaceutically-acceptable salt, or biohydrolyzable alkoxyamide, ester, acyloxyamide, or imide thereof. Also provided are compounds, pharmaceutical compositions and methods of treating diseases characterized by metalloprotease activity using these compounds or the pharmaceutical compositions containing them.
摘要翻译：目的：提供可用于治疗与不想要的金属蛋白酶活性相关的疾病，病症或病症的组合物。构成：提供可用作金属蛋白酶抑制剂的化合物，其有效治疗以过量的分解结构蛋白质的金属蛋白酶活性为特征的病症。特别地，提供具有根据式（I）的结构的化合物或其旋光异构体，非对映异构体或对映异构体或其药学上可接受的盐或生物可水解的烷氧基酰胺，酯，酰氧基酰胺或其酰亚胺。还提供了使用这些化合物或含有它们的药物组合物治疗以金属蛋白酶活性为特征的疾病的化合物，药物组合物和方法。

6. 发明公开

KR1020000035916A 스피로시클릭 메탈로프로테아제 저해제 失效
标题翻译：螺旋金属蛋白酶抑制剂
公开(公告)号：KR1020000035916A
公开(公告)日：2000-06-26
申请号：KR1019997001652
申请日：1997-08-22
申请人： 더 프록터 앤드 갬블 캄파니
发明人： 왕제 , 암스테드네일그레고리 , 브레들리림마샌들러 , 내쳐스마이클죠지 , 드비즈워나쓰 , 피쿨스태니슬로 , 타이워예툰데올라비지
IPC分类号： C07D495/10
CPC分类号： C07D471/10 , C07D209/96 , C07D491/10 , C07D495/10
摘要： PURPOSE: Compounds useful as metalloprotease inhibitors are provided which are effective in treating conditions characterized by excess activity of these enzymes. CONSTITUTION: Compounds of formula (I), or an optical isomer, diastereomer or elastomer thereof, or a pharmaceutically-acceptable salt, or biohydrolyzable amide, ester, or imide thereof are useful as inhibitors of metalloproteases. Also provided are pharmaceutical compositions and methods of treating diseases, disorders and conditions characterized by metalloprotease activity using these compounds or the pharmaceutical compositions containing them.
摘要翻译：目的：提供可用作金属蛋白酶抑制剂的化合物，其有效治疗以这些酶的过量活性为特征的病症。构成：式（I）化合物或其旋光异构体，非对映异构体或弹性体，或其药学上可接受的盐或可生物水解的酰胺，酯或酰亚胺可用作金属蛋白酶的抑制剂。还提供了使用这些化合物或含有它们的药物组合物治疗以金属蛋白酶活性为特征的疾病，病症和病症的药物组合物和方法。

7. 发明授权

KR100339296B1 헤테로고리성 메탈로프로테아제 억제제 失效
标题翻译：杂环金属蛋白酶抑制剂
公开(公告)号：KR100339296B1
公开(公告)日：2002-06-03
申请号：KR1019997001659
申请日：1997-08-22
申请人： 더 프록터 앤드 갬블 캄파니
发明人： 드비즈워나쓰 , 네이쳐스마이클죠지 , 피쿨스태니슬로 , 암스테드네일그레고리 , 매튜랜달스트라이커 , 타이워예툰데올라비지 , 쳉멘얀
IPC分类号： C07D243/08
CPC分类号： C07D265/30 , C07D223/06 , C07D241/04 , C07D241/08 , C07D279/12 , C07D281/00 , C07D281/06 , C07D401/06 , C07D401/12 , C07D405/06 , C07D409/06 , C07D413/06 , C07D417/12 , Y02P20/582
摘要： 본발명은메탈로프로테아제의억제제로서유용한, 상기청구항에기재된바와같은하기화학식 (I) 의화합물, 이의광학이성질체, 부분입체이성질체또는거울상이성질체, 또는이의약제학적으로허용가능한염, 생체내분해가능한아미드, 에스테르또는이미드에관한것이다. 또한, 본발명은상기화합물을이용한메탈로프로테아제활성을특징으로하는질병, 장애및 증상의치료방법및 약학조성물에관한것이다: [화학식 I]

8. 发明授权

KR100326611B1 스피로시클릭 메탈로프로테아제 저해제 失效
标题翻译：螺旋金属蛋白酶抑制剂
公开(公告)号：KR100326611B1
公开(公告)日：2002-03-02
申请号：KR1019997001652
申请日：1997-08-22
申请人： 더 프록터 앤드 갬블 캄파니
发明人： 왕제 , 암스테드네일그레고리 , 브레들리림마샌들러 , 내쳐스마이클죠지 , 드비즈워나쓰 , 피쿨스태니슬로 , 타이워예툰데올라비지
IPC分类号： C07D495/10
CPC分类号： C07D471/10 , C07D209/96 , C07D491/10 , C07D495/10
摘要： 본발명은청구범위에기술된바와같이메탈로프로테아제의저해제로서유용한하기화학식 (I) 의화합물, 또는그의광학이성질체, 부분입체이성질체또는거울상이성질체, 또는그의약제학적으로허용가능한염, 또는생체가수분해가능한아미드, 에스테르, 또는이미드를제공한다. 또한, 이들화합물또는이들을함유하는약제학적조성물을이용하여, 메탈로프로테아제활성을특징으로하는질환, 장애및 상태를치료하는약제학적조성물및 방법을설명하고있다.

9. 发明公开

KR1020000035922A 치환된 시클릭 아민 메탈로프로테아제 저해제 失效
标题翻译：取代的循环胺金属蛋白酶抑制剂
公开(公告)号：KR1020000035922A
公开(公告)日：2000-06-26
申请号：KR1019997001658
申请日：1997-08-22
申请人： 더 프록터 앤드 갬블 캄파니
发明人： 네이쳐스마이클죠지 , 드비즈워나쓰 , 피쿨스태니슬로 , 암스테드네일그레고리 , 북랜드로저군나드 , 타이워예툰데올라비지 , 쳉멘얀
IPC分类号： C07D207/48
CPC分类号： C07D207/42
摘要： PURPOSE: Provided are compositions which are useful for treatment of diseases, disorders or conditions associated with unwanted metalloprotease activity. CONSTITUTION: Provides are compounds which are useful as inhibitors of metalloproteases, and which are effective in treating conditions characterized by excess activity of these enzymes. In particular, the present invention relates to a compound having a structure according to formula (I). Wherein Ar is alkyl, heteroalkyl, aryl or heteroaryl, substituted or unsubstituted; R1 is OH, alkoxy, NHOR2, where R2 is hydrogen or alkyl; W is one or more of hydrogen, lower alkyl or an alkylene bridge; Y is independently one or more of hydroxy, SR3, SOR4, SO2R5, alkoxy, amino, wherein amino is of formula NR6,R7, wherein R6 and R7 are independently chosen from hydrogen, alkyl, heteroalkyl, heteroaryl, aryl, OR3, SO2Rg, COR9, CSR10, PO(R11)2; and R3 is hydrogen, alkyl, aryl, heteroaryl; R4 is alkyl, aryl, heteroaryl; R8 is alkyl, aryl, heteroaryl, heteroalkyl, amino, alkylamino, dialkylamino, arylamino, diarylamino and alkylarylamino; Rg is hydrogen, alkoxy, aryloxy, heteroaryloxy, alkyl, aryl, heteroaryl, heteroalkyl, amino, alkylamino, dialkylamino, arylamino and alkylarylamino; Rlo is alkyl, aryl, heteroaryl, heteroalkyl, amino, alkylamino, dialkylamino, arylamino, diarylamino and alkylarylamino; R1 1 is alkyl, aryl, heteroaryl, heteroalkyl; Z is hydrogen, hydroxy, alkyl, alkylene or heteroalkylene; n is 1-3. Also provided are compounds, pharmaceutical compositions and methods of treating diseases characterized by metalloprotease activity using these compounds or the pharmaceutical compositions containing them
摘要翻译：目的：提供可用于治疗与不想要的金属蛋白酶活性相关的疾病，病症或病症的组合物。构成：提供可用作金属蛋白酶抑制剂的化合物，其有效治疗以这些酶的过量活性为特征的病症。特别地，本发明涉及具有式（I）结构的化合物。其中Ar为烷基，杂烷基，芳基或杂芳基，取代或未取代的; R1是OH，烷氧基，NHOR2，其中R2是氢或烷基; W是氢，低级烷基或亚烷基桥中的一个或多个; Y独立地是羟基，SR3，SOR4，SO2R5，烷氧基，氨基，其中氨基具有式NR6，R7的一个或多个，其中R6和R7独立地选自氢，烷基，杂烷基，杂芳基，芳基，OR3，SO2Rg， COR9，CSR10，PO（R11）2; 并且R 3是氢，烷基，芳基，杂芳基; R4是烷基，芳基，杂芳基; R8是烷基，芳基，杂芳基，杂烷基，氨基，烷基氨基，二烷基氨基，芳基氨基，二芳基氨基和烷基芳基氨基; R g是氢，烷氧基，芳氧基，杂芳氧基，烷基，芳基，杂芳基，杂烷基，氨基，烷基氨基，二烷基氨基，芳基氨基和烷基芳基氨基; R 12是烷基，芳基，杂芳基，杂烷基，氨基，烷基氨基，二烷基氨基，芳基氨基，二芳基氨基和烷基芳基氨基; R 1是烷基，芳基，杂芳基，杂烷基; Z是氢，羟基，烷基，亚烷基或杂亚烷基; n为1-3。还提供了使用这些化合物或含有它们的药物组合物治疗以金属蛋白酶活性为特征的疾病的化合物，药物组合物和方法

10. 发明公开

KR1020000035920A 헤테로고리성 메탈로프로테아제 저해제 无效
标题翻译：杂环金属蛋白酶抑制剂
公开(公告)号：KR1020000035920A
公开(公告)日：2000-06-26
申请号：KR1019997001656
申请日：1997-08-22
申请人： 더 프록터 앤드 갬블 캄파니
发明人： 피쿨스태니슬로 , 맥도우-던햄켈리린 , 드비즈워나쓰 , 타이워예툰데올라비지 , 암스테드네일그레고리 , 브래들리림마샌들러 , 네어쳐스마이클죠지 , 쿱스토마스리
IPC分类号： C07D239/06
CPC分类号： C07D239/06 , C07D243/08 , C07D281/06 , C07D403/12 , C07D409/12 , C07D409/14 , C07D413/14 , C07D487/06
摘要： PURPOSE: Provided is Compounds useful for the treatment of conditions and diseases which are characterized by unwanted MP activity, potent inhibitors of metalloproteases, pharmaceutical compositions comprising such inhibitors and a method of treatment for metalloprotease related maladies. CONSTITUTION: The compounds of the invention are useful as inhibitors of metalloproteases, preferably a matrix metalloproteases, and which are effective in treating conditions characterized by excess activity of these enzymes. In particular, the compound having a structure according to Formula (I). The inhibitors of the invention can be targeted to specific locations where the metalloprotease is accumulated by using targeting ligands. The compounds are relatively small, they are advantageously coupled to neutral carriers such as the conventionally used keyhole limpet hemocyanin (KLH) or serum albumin carriers.
摘要翻译：目的：提供可用于治疗以不需要的MP活性为特征的病症和疾病的化合物，金属蛋白酶的有效抑制剂，包含这种抑制剂的药物组合物和金属蛋白酶相关疾病的治疗方法。构成：本发明的化合物可用作金属蛋白酶抑制剂，优选基质金属蛋白酶，并且其有效治疗以这些酶的过量活性为特征的病症。特别是具有式（I）结构的化合物。本发明的抑制剂可以靶向通过使用靶向配体积聚金属蛋白酶的特定位置。化合物相对较小，它们有利地与中性载体偶联，例如常规使用的钥孔血蓝蛋白（KLH）或血清白蛋白载体。

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