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1. 发明申请

WO1995012603A1 MATRIX METALLOPROTEASE INHIBITORS________________________________ 审中-公开
公开(公告)号：WO1995012603A1
公开(公告)日：1995-05-11
申请号：PCT/US1994012214
申请日：1994-11-03
申请人： SYNTEX (U.S.A.) INC.
发明人： SYNTEX (U.S.A.) INC. , CASTELHANO, Arlindo, L. , YUAN, Zhengyu , HORNE, Stephen , LIAK, Teng, J.
IPC分类号： C07F09/30
CPC分类号： C07D213/75 , C07C237/22 , C07C237/42 , C07C255/57 , C07C255/60 , C07C259/06 , C07C279/14 , C07C311/46 , C07C317/40 , C07C323/59 , C07C323/60 , C07C323/63 , C07C327/12 , C07C327/32 , C07C2601/14 , C07C2603/18 , C07D263/26 , C07D295/13 , C07F9/301 , C07F9/306 , C07F9/3211 , C07F9/3241 , C07F9/4816 , C07F9/58 , C07F9/60 , C07F9/65583
摘要： This invention is directed to compounds of formula (I): wherein R is mercapto, acetylthio, carboxy, hydroxycarbamoyl, alkoxycarbonyl, aryloxycarbonyl, aralkoxycarbonyl, benzyloxycarbamoyl or (i) (where R is optionally substituted aryl, wherein the aryl group is quinol-2-yl, naphth-1-yl, naphth-2-yl, pyridyl or phenyl); R is alkyl, aralkyl or cycloalkylalkyl; R is cycloalkyl, alkyl (optionally substituted by cycloalkyl, hydroxy, mercapto, alkylthio, aralkoxy, carboxy, amino, alkylamino, guanidino, carbamoyl, pyridyl or indolyl), or aralkyl (optionally substituted by hydroxy, carboxy, alkyl or alkoxy); R is nitro, amino, cyano, hydroxy, alkoxy, carboxy, alkoxycarbonyl, alkylsulfonyl, haloalkyl, alkoxycarbonylalkyl, tetrazolyl, carbamoyl (optionally substituted by alkyl or dialkylaminoalkyl), or aminosulfonyl (optionally substituted by alkyl); and R is hydrogen, halo or hydroxy; as single stereoisomers or as mixtures thereof; or the pharmaceutically acceptable salts thereof. These compounds are useful in inhibiting matrix metalloprotease activity in mammals.
摘要翻译：本发明涉及式（I）的化合物：其中R 1是巯基，乙酰硫基，羧基，羟基氨基甲酰基，烷氧基羰基，芳氧基羰基，芳烷氧基羰基，苄氧基氨基甲酰基或（i）（其中R 6是任选取代的芳基，芳基是喹啉-2-基，萘-1-基，萘-2-基，吡啶基或苯基）; R 2是烷基，芳烷基或环烷基烷基; R 3是环烷基（任选被环烷基，羟基，巯基，烷硫基，芳烷氧基，羧基，氨基，烷基氨基，胍基，氨基甲酰基，吡啶基或吲哚基取代）或芳烷基（任选被羟基，羧基，烷基或烷氧基取代）; R 4为硝基，氨基，氰基，羟基，烷氧基，羧基，烷氧基羰基，烷基磺酰基，卤代烷基，烷氧基羰基烷基，四唑基，氨基甲酰基（任选被烷基或二烷基氨基烷基取代）或氨基磺酰基（任选被烷基取代）和R 5是氢，卤素或羟基; 作为单一立体异构体或其混合物; 或其药学上可接受的盐。这些化合物可用于抑制哺乳动物的基质金属蛋白酶活性。

2. 发明申请

WO1996023791A1 BRIDGED INDOLES AS MATRIX METALLOPROTEASE INHIBITORS 审中-公开
标题翻译：作为基质金属蛋白酶抑制剂的桥连
公开(公告)号：WO1996023791A1
公开(公告)日：1996-08-08
申请号：PCT/US1996001506
申请日：1996-02-02
申请人： SYNTEX (U.S.A.) INC.
发明人： SYNTEX (U.S.A.) INC. , CASTELHANO, Arlindo, L. , LIAK, Teng, J. , HORNE, Stephen , YUAN, Zhengyu , KRANTZ, Alexander , CHEN, Jian, Jeffrey , VAN WART, Harold , CANNON, Paul, D.
IPC分类号： C07D487/08
CPC分类号： C07D487/04 , C07D487/08 , C07F9/6561
摘要： Compounds of formula (I) as single stereoisomers or mixtures thereof and their pharmaceutically acceptable salts inhibit matrix metalloproteases, such as interstitial collagenases, and are useful in the treatment of mammals having disease states alleviated by the inhibition of such matrix metalloproteases, for example arthritic diseases or bone resorption diseases, such as osteoporosis.
摘要翻译：作为单一立体异构体或其混合物的式（I）化合物及其药学上可接受的盐抑制基质金属蛋白酶，例如间质胶原酶，并且可用于治疗具有通过抑制这种基质金属蛋白酶减轻的疾病状态的哺乳动物，例如关节炎疾病或骨吸收疾病，如骨质疏松症。

3. 发明申请

WO1996016027A1 MATRIX METALLOPROTEASE INHIBITORS 审中-公开
标题翻译： MATRIX METALLOPROTEASE抑制剂
公开(公告)号：WO1996016027A1
公开(公告)日：1996-05-30
申请号：PCT/US1995015530
申请日：1995-11-21
申请人： SYNTEX (U.S.A.) INC. , AGOURON PHARMACEUTICALS, INC.
发明人： SYNTEX (U.S.A.) INC. , AGOURON PHARMACEUTICALS, INC. , CASTELHANO, Arlindo, L. , BENDER, Steven, L. , DEAL, Judith, G. , HORNE, Stephen , LIAK, Teng, J. , YUAN, Zhengyu
IPC分类号： C07C259/06
CPC分类号： C07D213/75 , C07C237/22 , C07C237/42 , C07C255/57 , C07C255/60 , C07C259/06 , C07C279/14 , C07C311/46 , C07C317/40 , C07C323/59 , C07C323/60 , C07C323/63 , C07C327/12 , C07C327/32 , C07C2601/14 , C07C2603/18 , C07D263/26 , C07D295/13 , C07F9/301 , C07F9/306 , C07F9/3211 , C07F9/3241 , C07F9/4816 , C07F9/58 , C07F9/60 , C07F9/65583
摘要： Compounds of formula (I) and their pharmaceutically acceptable salts inhibit matrix metalloproteases, such as stromelysin, gelatinase, matrilysin and collagenase, and are useful in the treatment of mammals having disease-states alleviated by the inhibition of such matrix metalloproteases.
摘要翻译：式（I）化合物及其药学上可接受的盐抑制基质金属蛋白酶，例如溶基质溶解素，明胶酶，基质溶素和胶原酶，并且可用于治疗通过抑制这种基质金属蛋白酶而减轻疾病的哺乳动物。

4. 发明申请

WO1995004735A1 MATRIX METALLOPROTEASE INHIBITORS 审中-公开
标题翻译： MATRIX METALLOPROTEASE抑制剂
公开(公告)号：WO1995004735A1
公开(公告)日：1995-02-16
申请号：PCT/US1994008510
申请日：1994-07-27
申请人： SYNTEX (U.S.A.) INC.
发明人： SYNTEX (U.S.A.) INC. , CASTELHANO, Arlindo, L. , LIAK, Teng, J. , HORNE, Stephen , YUAN, Zhengyo , KRANTZ, Alexander
IPC分类号： C07D487/04
CPC分类号： C07D487/04 , C07D487/08 , C07F9/6561
摘要： Compounds of formula (I), wherein the dashed lines denote optional double bonds; and when n is 1, 2 or 3; m is 3 or 4; A is -CH2-; R is a) -CH2-R where R is mercapto, acetylthio, carboxy, hydroxyaminocarbonyl, N-hydroxyformamidomethyl, alkoxycarbonyl, aryloxycarbonyl, aralcoxycarbonyl, benzyloxyaminocarbonyl, or (i), where R is optionally substituted aryl, wherein the aryl group is quinol-2-yl, naphth-1-yl, naphth-2-yl, pyridyl or phenyl; b) -CH(R )-R where R is alkyl, hydroxy, amino, aminomethyl, alkylsulphonylamidomethyl, aralkylsulphonylamidomethyl, alkoxycarbonyl, alkoxycarbonylaminomethyl, alkylaminocarbonylamidomethyl, benzoxazoleaminomethyl, aminocarbonyl, or carboxy; and R is carboxy, hydroxyaminocarbonyl, alkoxycarbonyl or aralkoxycarbonyl; c) -NH-CH(R ) -R where R is hydrogen, alkyl or aralkyl, and R is carboxy, alkoxycarbonyl, aralkoxycarbonyl, phosphonyl or dialkylphosphonyl; R is alkyl, cycloalkyl, cycloalkylalkyl or aralkyl; and R is hydrogen, halo, alkyl or alkoxy; or when n is 2 or 3; m is 3 or 4; A is -N(R )-, where R is hydrogen or alkyl; and R , R and R are as defined above; or when n is 0; m is 4, 5 or 6; A is -CH(R )-, where R is carboxy, alkoxycarbonyl or optionally substituted carbamoyl; and R , R and R are as defined above; as single stereoisomers or mixtures thereof; or pharmaceutically acceptable salts thereof; are useful in inhibiting matrix metalloprotease activity in mammals.
摘要翻译：式（I）的化合物，其中虚线表示任选的双键; 当n为1,2或3时; m为3或4; A是-CH 2 - ; R 1是a）-CH 2 -R 4，其中R 4是巯基，乙酰硫基，羧基，羟基氨基羰基，N-羟基甲酰胺基甲基，烷氧基羰基，芳氧基羰基，芳氧羰基，苄氧基氨基羰基或（i），其中R 6，是任选取代的芳基，其中芳基是喹啉-2-基，萘-1-基，萘-2-基，吡啶基或苯基; b）-CH（R 7）-R 8，其中R 7是烷基，羟基，氨基，氨基甲基，烷基磺酰基氨基甲基，芳烷基磺酰氨基甲基，烷氧基羰基，烷氧基羰基氨基甲基，烷基氨基羰基氨基甲基，苯并恶唑氨基甲基，氨基羰基或羧基; 和R 8是羧基，羟基氨基羰基，烷氧基羰基或芳烷氧基羰基; c）-NH-CH（R 9）-R 10其中R 9是氢，烷基或芳烷基，R 10是羧基，烷氧基羰基，芳烷氧基羰基，膦酰基或二烷基膦酰基; R 2是烷基，环烷基，环烷基烷基或芳烷基; 和R 3是氢，卤素，烷基或烷氧基; 或当n为2或3时; m为3或4; A是-N（R 11） - ，其中R 11是氢或烷基; 且R 1，R 2和R 3如上定义; 或当n为0时; m为4,5或6; A是-CH（R 12） - ，其中R 12是羧基，烷氧基羰基或任选取代的氨基甲酰基; 且R 1，R 2和R 3如上定义; 作为单一立体异构体或其混合物; 或其药学上可接受的盐; 可用于抑制哺乳动物的基质金属蛋白酶活性。

5. 发明公开

EP0726903A1 MATRIX METALLOPROTEASE INHIBITORS-------------------------------- 有权
标题翻译：金属基蛋白酶抑制剂
公开(公告)号：EP0726903A1
公开(公告)日：1996-08-21
申请号：EP94932023.0
申请日：1994-11-03
申请人： SYNTEX (U.S.A.) INC.
发明人： CASTELHANO, Arlindo, L. , YUAN, Zhengyu , HORNE, Stephen , LIAK, Teng, J.
IPC分类号： C07D213 , A61K31 , A61P27 , A61P29 , A61P35 , A61P43 , C07C51 , C07C53 , C07C57 , C07C67 , C07C69 , C07C233 , C07C237 , C07C255 , C07C259 , C07C271 , C07C279 , C07C311 , C07C317 , C07C323 , C07C327 , C07D209 , C07D263 , C07D295 , C07F9
CPC分类号： C07D213/75 , C07C237/22 , C07C237/42 , C07C255/57 , C07C255/60 , C07C259/06 , C07C279/14 , C07C311/46 , C07C317/40 , C07C323/59 , C07C323/60 , C07C323/63 , C07C327/12 , C07C327/32 , C07C2601/14 , C07C2603/18 , C07D263/26 , C07D295/13 , C07F9/301 , C07F9/306 , C07F9/3211 , C07F9/3241 , C07F9/4816 , C07F9/582 , C07F9/60 , C07F9/65583

6. 发明授权

EP0726903B1 MATRIX METALLOPROTEASE INHIBITORS 有权
标题翻译： MATRIX METALLPROTEASE INHIBITOREN
公开(公告)号：EP0726903B1
公开(公告)日：1997-07-16
申请号：EP94932023.8
申请日：1994-11-03
申请人： SYNTEX (U.S.A.) INC.
发明人： CASTELHANO, Arlindo, L. , YUAN, Zhengyu , HORNE, Stephen , LIAK, Teng, J.
IPC分类号： C07F9/30 , A61K31/66 , C07F9/60 , C07F9/58 , C07C233/47 , C07C255/60 , C07C323/52 , C07C327/22 , C07D209/20 , C07C259/06
CPC分类号： C07D213/75 , C07C237/22 , C07C237/42 , C07C255/57 , C07C255/60 , C07C259/06 , C07C279/14 , C07C311/46 , C07C317/40 , C07C323/59 , C07C323/60 , C07C323/63 , C07C327/12 , C07C327/32 , C07C2601/14 , C07C2603/18 , C07D263/26 , C07D295/13 , C07F9/301 , C07F9/306 , C07F9/3211 , C07F9/3241 , C07F9/4816 , C07F9/582 , C07F9/60 , C07F9/65583
摘要： This invention is directed to compounds of formula (I): wherein R1 is mercapto, acetylthio, carboxy, hydroxycarbamoyl, alkoxycarbonyl, aryloxycarbonyl, aralkoxycarbonyl, benzyloxycarbamoyl or (i) (where R6 is optionally substituted aryl, wherein the aryl group is quinol-2-yl, naphth-1-yl, naphth-2-yl, pyridyl or phenyl); R2 is alkyl, aralkyl or cycloalkylalkyl; R3 is cycloalkyl, alkyl (optionally substituted by cycloalkyl, hydroxy, mercapto, alkylthio, aralkoxy, carboxy, amino, alkylamino, guanidino, carbamoyl, pyridyl or indolyl), or aralkyl (optionally substituted by hydroxy, carboxy, alkyl or alkoxy); R4 is nitro, amino, cyano, hydroxy, alkoxy, carboxy, alkoxycarbonyl, alkylsulfonyl, haloalkyl, alkoxycarbonylalkyl, tetrazolyl, carbamoyl (optionally substituted by alkyl or dialkylaminoalkyl), or aminosulfonyl (optionally substituted by alkyl); and R5 is hydrogen, halo or hydroxy; as single stereoisomers or as mixtures thereof; or the pharmaceutically acceptable salts thereof. These compounds are useful in inhibiting matrix metalloprotease activity in mammals.
摘要翻译：本发明涉及式（I）的化合物：其中R 1为巯基，乙酰硫基，羧基，羟基氨基甲酰基，烷氧基羰基，芳氧基羰基，芳烷氧基羰基，苄氧基氨基甲酰基或（i）（其中R 6为任选取代的芳基，芳基是喹啉-2-基，萘-1-基，萘-2-基，吡啶基或苯基）; R 2是烷基，芳烷基或环烷基烷基; R 3是环烷基（任选被环烷基，羟基，巯基，烷硫基，芳烷氧基，羧基，氨基，烷基氨基，胍基，氨基甲酰基，吡啶基或吲哚基取代）或芳烷基（任选被羟基，羧基，烷基或烷氧基）; R 4是硝基，氨基，氰基，羟基，烷氧基，羧基，烷氧基羰基，烷基磺酰基，卤代烷基，烷氧基羰基烷基，四唑基，氨基甲酰基（任选被烷基或二烷基氨基烷基取代）或氨基磺酰基（任选被烷基取代）和R 5是氢，卤素或羟基; 作为单一立体异构体或其混合物; 或其药学上可接受的盐。这些化合物可用于抑制哺乳动物中的基质金属蛋白酶活性。

7. 发明公开

EP0712403A1 MATRIX METALLOPROTEASE INHIBITORS 失效
标题翻译：基质金属蛋白酶抑制剂
公开(公告)号：EP0712403A1
公开(公告)日：1996-05-22
申请号：EP94925699.0
申请日：1994-07-27
申请人： SYNTEX (U.S.A.) INC.
发明人： CASTELHANO, Arlindo, L. , LIAK, Teng, J. , HORNE, Stephen , YUAN, Zhengyo , KRANTZ, Alexander
IPC分类号： A61K31 , A61P1 , A61P29 , A61P35 , A61P43 , C07D487 , C07D498 , C07F9
CPC分类号： C07D487/04 , C07D487/08 , C07F9/6561

8. 发明公开

EP0807114A1 BRIDGED INDOLES AS MATRIX METALLOPROTEASE INHIBITORS 失效
标题翻译： BRIDGED INDOLES作为基质金属蛋白酶抑制剂
公开(公告)号：EP0807114A1
公开(公告)日：1997-11-19
申请号：EP96904563.0
申请日：1996-02-02
申请人： SYNTEX (U.S.A.) INC.
发明人： CASTELHANO, Arlindo, L. , LIAK, Teng, J. , HORNE, Stephen , YUAN, Zhengyu , KRANTZ, Alexander , CHEN, Jian, Jeffrey , VAN WART, Harold , CANNON, Paul, D.
IPC分类号： A61K31 , A61P1 , A61P3 , A61P19 , A61P29 , A61P35 , A61P43 , C07D487 , C07D498 , C07F9
CPC分类号： C07D487/04 , C07D487/08 , C07F9/6561
摘要： Compounds of formula (I) as single stereoisomers or mixtures thereof and their pharmaceutically acceptable salts inhibit matrix metalloproteases, such as interstitial collagenases, and are useful in the treatment of mammals having disease states alleviated by the inhibition of such matrix metalloproteases, for example arthritic diseases or bone resorption diseases, such as osteoporosis.
摘要翻译：作为单一立体异构体或其混合物的式（I）化合物及其药学上可接受的盐抑制基质金属蛋白酶如间质胶原酶，并且可用于治疗具有通过抑制此类基质金属蛋白酶缓解疾病状态的哺乳动物，例如关节炎疾病或骨吸收疾病，如骨质疏松症。

9. 发明授权

EP0712403B1 MATRIX METALLOPROTEASE INHIBITORS 失效
标题翻译：基质金属蛋白酶抑制剂
公开(公告)号：EP0712403B1
公开(公告)日：1997-09-10
申请号：EP94925699.4
申请日：1994-07-27
申请人： SYNTEX (U.S.A.) INC.
发明人： CASTELHANO, Arlindo, L. , LIAK, Teng, J. , HORNE, Stephen , YUAN, Zhengyo , KRANTZ, Alexander
IPC分类号： C07D487/08 , A61K31/395 , C07F9/30
CPC分类号： C07D487/04 , C07D487/08 , C07F9/6561
摘要： Compounds of formula (I), wherein the dashed lines denote optional double bonds; and when n is 1, 2 or 3; m is 3 or 4; A is -CH2-; R1 is a) -CH¿2-R?4 where R4 is mercapto, acetylthio, carboxy, hydroxyaminocarbonyl, N-hydroxyformamidomethyl, alkoxycarbonyl, aryloxycarbonyl, aralcoxycarbonyl, benzyloxyaminocarbonyl, or (i), where R6 is optionally substituted aryl, wherein the aryl group is quinol-2-yl, naphth-1-yl, naphth-2-yl, pyridyl or phenyl; b) -CH(R7)-R8 where R7 is alkyl, hydroxy, amino, aminomethyl, alkylsulphonylamidomethyl, aralkylsulphonylamidomethyl, alkoxycarbonyl, alkoxycarbonylaminomethyl, alkylaminocarbonylamidomethyl, benzoxazoleaminomethyl, aminocarbonyl, or carboxy; and R8 is carboxy, hydroxyaminocarbonyl, alkoxycarbonyl or aralkoxycarbonyl; c) -NH-CH(R9) -R10 where R9 is hydrogen, alkyl or aralkyl, and R10 is carboxy, alkoxycarbonyl, aralkoxycarbonyl, phosphonyl or dialkylphosphonyl; R2 is alkyl, cycloalkyl, cycloalkylalkyl or aralkyl; and R3 is hydrogen, halo, alkyl or alkoxy; or when n is 2 or 3; m is 3 or 4; A is -N(R11)-, where R11 is hydrogen or alkyl; and R?1, R2 and R3¿ are as defined above; or when n is 0; m is 4, 5 or 6; A is -CH(R12)-, where R12 is carboxy, alkoxycarbonyl or optionally substituted carbamoyl; and R?1, R2 and R3¿ are as defined above; as single stereoisomers or mixtures thereof; or pharmaceutically acceptable salts thereof; are useful in inhibiting matrix metalloprotease activity in mammals.

10. 发明公开

EP0793643A1 MATRIX METALLOPROTEASE INHIBITORS 失效
标题翻译：基质金属蛋白酶抑制剂
公开(公告)号：EP0793643A1
公开(公告)日：1997-09-10
申请号：EP95941493.0
申请日：1995-11-21
申请人： SYNTEX (U.S.A.) INC. , AGOURON PHARMACEUTICALS, INC.
发明人： CASTELHANO, Arlindo, L. , BENDER, Steven, L. , DEAL, Judith, G. , HORNE, Stephen , LIAK, Teng, J. , YUAN, Zhengyu
IPC分类号： C07D213 , A61K31 , A61K38 , A61P1 , A61P3 , A61P27 , A61P29 , A61P35 , A61P43 , C07C51 , C07C53 , C07C57 , C07C67 , C07C69 , C07C231 , C07C233 , C07C237 , C07C255 , C07C259 , C07C271 , C07C279 , C07C311 , C07C317 , C07C323 , C07C327 , C07D205 , C07D209 , C07D263 , C07D295 , C07D307 , C07D333 , C07F9 , C07K5
CPC分类号： C07D213/75 , C07C237/22 , C07C237/42 , C07C255/57 , C07C255/60 , C07C259/06 , C07C279/14 , C07C311/46 , C07C317/40 , C07C323/59 , C07C323/60 , C07C323/63 , C07C327/12 , C07C327/32 , C07C2601/14 , C07C2603/18 , C07D263/26 , C07D295/13 , C07F9/301 , C07F9/306 , C07F9/3211 , C07F9/3241 , C07F9/4816 , C07F9/582 , C07F9/60 , C07F9/65583
摘要： Compounds of formula (I) and their pharmaceutically acceptable salts inhibit matrix metalloproteases, such as stromelysin, gelatinase, matrilysin and collagenase, and are useful in the treatment of mammals having disease-states alleviated by the inhibition of such matrix metalloproteases.
摘要翻译：式（I）化合物及其药学上可接受的盐抑制基质金属蛋白酶，例如基质溶素，明胶酶，基质溶解素和胶原酶，并且可用于治疗具有通过抑制此类基质金属蛋白酶而减轻疾病状态的哺乳动物。

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