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1. 发明公开

EP0230266A3 Functionalized peptidyl aminodiols and -triols 失效
标题翻译：功能性磷酸二肽和 -
公开(公告)号：EP0230266A3
公开(公告)日：1990-01-17
申请号：EP87100422.2
申请日：1987-01-15
申请人： ABBOTT LABORATORIES
发明人： Rosenberg, Saul Howard , Plattner, Jacob John , Luly, Jay Richard
IPC分类号： C07K5/06 , C07K5/02 , C07K5/08 , C07D233/64 , A61K31/415 , A61K37/02 , A61K37/64
CPC分类号： C07D233/64 , A61K38/00 , C07K5/0227 , C07K5/06043 , C07K5/06078 , C07K5/0806
摘要： The invention relates to renin inhibiting compounds of the formula
wherein A is hydrogen; loweralkyl; arylalkyl; OR₈ or SR₈ wherein R₈ is hydrogen, loweralkyl or aminoalkyl; NR₉R₁₀ wherein R₉ and R₁₀ are independently selected from hydrogen, loweralkyl, aminoalkyl, cyanoalkyl and hydroxyalkyl;
wherein B is NH, alkylamino, S, O, CH₂ or CHOH and R₁₁ is loweralkyl, cycloalkyl, aryl, arylalkyl, alkoxy, alkenyloxy, hydroxyalkoxy, dihydroxyalkoxy, arylalkoxy, arylalkoxyalkyl, amino, alkylamino, dialkylamino, (hydroxyalkyl)(alkyl)amino, (dihydroxyalkyl)(alkyl)amino, carboxylic acid-substituted alkyl, alkoxycarbonylalkyl, aminoalkyl, N-protected aminoalkyl, alkylaminoalkyl, dialkylaminoalkyl, (N-protected) alkyl)aminoalkyl, (heterocyclic)alkyl or a substituted or unsubstituted heterocyclic; R₁ is loweralkyl, cycloalkylmethyl, benzyl, α-methylbenzyl, α, α-dimethylbenzyl, 4-methoxybenzyl, halobenzyl, (1-naphthyl)methyl, (2-naphthyl)methyl, (4-imidazoyl)methyl, phenethyl, phenoxy, thiophenoxy or anilino; provided if R₁ is phenoxy, thiophenoxy or anilino, B is CH₂ or CHOH or A is hydrogen; R₃ is loweralkyl, benzyl or heterocyclic ring-substituted methyl; R₄ is loweralkyl, cycloalkyl- methyl or benzyl; R₂, R₅ and R₆ are independently hydrogen or loweralkyl; X is O, NH or S; R₇ is hydrogen, loweralkyl, alkanoyl, alkylsulfonyl.
wherein R₁₂ and R₁₃ are independently hydrogen or loweralkyl, n is 0-2 and R₁₄ is substituted or unsubstituted penyl or heterocyclic; or XR₇ together are loweralkylsulfonyl, N₃ or Cl, and pharmaceutically acceptable salts thereof.

2. 发明公开

EP0172346A2 Renin inhibiting compounds 失效
标题翻译：肾素抑制化合物
公开(公告)号：EP0172346A2
公开(公告)日：1986-02-26
申请号：EP85107374.2
申请日：1985-06-18
申请人： ABBOTT LABORATORIES
发明人： Luly, Jay Richard , Dellaria, Joseph Fred , Plattner, John Jacob
IPC分类号： C07K5/00 , C07K5/06 , C07C103/30 , C07C103/50 , A61K31/16 , A61K37/64
CPC分类号： C07K5/06078 , A61K38/00 , C07K5/0227 , Y02P20/55 , Y10S530/86
摘要： The invention relates to renin inhibiting compounds of the formula

wherein A is an N-protecting group; n is 0 or 1; B is hydrogen, hydroxy NH, loweralkyl or arylalkyl; with the proviso that when A is an N-protecting group, B is NH and when n is 0, B is hydrogen, hydroxy, loweralkyl or arylalkyl; R,, R 3 and R 5 are loweralkyl or hydrophilic, lipophilic or aromatic amino acid side chains and may be the same or different; R 2 , R 4 , R 7 , R 8 and R 9 are hydrogen or loweralkyl and may be the same or different; X is CH 2 ; R B is loweralkyl, cycloalkyl, cycloalkylalkyl, aryl or arylalkyl; and X and R 6 when taken together may be a vinylic group.
摘要翻译：本发明涉及下式的肾素抑制化合物：其中A是N-保护基; n是0或1; B是氢，羟基NH，低级烷基或芳基烷基; 条件是当A是N-保护基团时，B是NH，并且当n是0时，B是氢，羟基，低级烷基或芳基烷基; R 1，R 3和R 5是低级烷基或亲水性，亲脂性或芳族氨基酸侧链，并且可以相同或不同; R2，R4，R7，R8和R9是氢或低级烷基并且可以相同或不同; X是CH2; RB是低级烷基，环烷基，环烷基烷基，芳基或芳基烷基; 并且X和R6一起时可以是乙烯基。

3. 发明公开

EP0229667A2 Peptidylaminodiols 失效
公开(公告)号：EP0229667A2
公开(公告)日：1987-07-22
申请号：EP87100424.8
申请日：1987-01-15
申请人： ABBOTT LABORATORIES
发明人： Luly, Jay Richard , Kempf, Dale John , Plattner, Jacob John
IPC分类号： C07K5/06 , C07K5/08 , C07K5/02 , C07D233/64 , C07C237/12 , A61K31/415 , A61K37/02 , A61K37/64 , A61K31/16
CPC分类号： C07D233/64 , A61K38/00 , C07K5/0202 , C07K5/0227 , C07K5/06026 , C07K5/06043 , C07K5/0606 , C07K5/06078 , C07K5/0806 , C07K5/0808 , C07K5/0821 , C07K5/0823 , Y02P20/55
摘要： A renin inhibiting compound of the formula:
wherein A is a substituent; W is C=O or CHOH; U is CH₂ or NR₂, provided that when W is CHOH then U is CH₂; R₁ is loweralkyl, cycloalkylmethyl, benzyl, 4-methoxybenzyl, halobenzyl, (1-naphthyl)methyl, (2-naphthyl)methyl, (4-imidazoyl)methyl, α, α -dimethylbenzyl, 1-benzyloxyethyl, phenethyl, phenoxy, thiophenoxy or anilino; R₂ is hydrogen or loweralkyl; R₃ is loweralkyl, [(alkoxy)alkoxy]alkyl, (thioalkoxy)alkyl, lowerakenyl, benzyl or heterocyclic ring substituted methyl; R₄ is loweralkyl, cycloalkylmethyl or benzyl; R₅ is vinyl, formyl, hydroxymethyl or hydrogen; R₇ is hydrogen or loweralkyl; R₈ and R₉ are independently selected from OH and NH₂; and R₆ is hydrogen, loweralkyl, vinyl or arylalkyl; provided that when R₅ and R₇ are both hydrogen and R₈ and R₉ are OH, the carbon bearing R₅ is of the "R" configuration and the carbon bearing R₆ is of the "S" configuration; or pharmaceutically acceptable salts or esters thereof. Also disclosed are renin inhibiting compositions, a method of treating hypertension, methods of making the renin inhibiting compounds and intermediates useful in making the renin inhibiting compounds.
摘要翻译：一种下式的肾素抑制化合物：其中A是取代基; W是C = O或CHOH; U是CH 2或NR 2，条件是当W是CHOH时，则U是CH 2; （1-萘基）甲基，（2-萘基）甲基，（4-咪唑基）甲基，α，α-二甲基苄基，1-苄氧基乙基，苯乙基，苯氧基，硫代苯氧基（低级烷基）或苯胺基; R 2是氢或低级烷基; R 3是低级烷基，[（烷氧基）烷氧基]烷基，（硫代烷氧基）烷基，低级链烯基，苄基或杂环取代的甲基; R 4是低级烷基，环烷基甲基或苄基; R 5是乙烯基，甲酰基，羟甲基或氢; R 7是氢或低级烷基; R 7和R 7独立地选自OH和NH 2; 和R 6是氢，低级烷基，乙烯基或芳基烷基; 条件是当R 5和R 7都是氢而R 7和R 7是OH时，带有R 5的碳是“R”构型，带有R 6的碳是“S”构型; 或其药学上可接受的盐或酯。还公开了肾素抑制组合物，治疗高血压的方法，制备肾素抑制化合物和中间体用于制备肾素抑制化合物的方法。

4. 发明公开

EP0189203A2 Peptidylaminodiols 失效
标题翻译： Peptidylaminodiole。
公开(公告)号：EP0189203A2
公开(公告)日：1986-07-30
申请号：EP86100917.3
申请日：1986-01-23
申请人： ABBOTT LABORATORIES
发明人： Luly, Jay Richard , Plattner, John Jacob , Rosenberg, Saul Howard , Fung, Anthony K.L.
IPC分类号： C07K5/06 , C07D233/64 , A61K37/64
CPC分类号： C07K5/06078 , A61K38/00 , C07K5/0227 , C07K5/06017 , C07K5/06139 , Y02P20/55
摘要： The invention relates to renin inhibiting compounds of the formula:
wherein R 10 is
A is hydrogen or an N-protecting group; w is 0 or 1; B is hydrogen, hydroxy, NH, N-alkyl, loweralkyl or arylalkyl; with the proviso that when w is 1, B is NH and when w is 0, B is hydrogen, hydroxy, loweralkyl or arylalkyl; R 1 is loweralkyl or lipophilic or aromatic or hydrophilic amino acid side chains; m is 1-3; n is 1-3; p is 1-3; q is 1-3; s is 1-3; t is 0-2; R 2 is hydrogen or loweralkyl; R 3 and R 4 are independently selected from loweralkyl, lipophilic or aromatic amino acid side chains; R 5 and R 7 are independently selected from hydrogen or loweralkyl; and R 6 is hydrogen, loweralkyl, vinyl, arylalkyl or wherein R 8 is hydrogen or loweralkyl, X is O, NH or S and R 9 is hydrogen, loweralkyl or alkanoyl or XR 9 together can be loweralkylsulfonyl, N 3 or Cl.
摘要翻译：本发明涉及下式的肾素抑制化合物：其中R 10是氢或N-保护基; w为0或1; B是氢，羟基，NH，N-烷基，低级烷基或芳基烷基; 条件是当w为1时，B为NH，当w为0时，B为氢，羟基，低级烷基或芳基烷基; R1是低级烷基或亲脂性或芳族或亲水氨基酸侧链; m为1-3; n为1-3; p为1-3; q为1-3; s是1-3; t为0-2; R2是氢或低级烷基; R3和R4独立地选自低级烷基，亲脂性或芳族氨基酸侧链; R5和R7独立地选自氢或低级烷基; 并且R 6是氢，低级烷基，乙烯基，芳烷基或其中R 8是氢或低级烷基，X是O，NH或S，R 9是氢，低级烷基或烷酰基或X R 9一起可以是低级烷基磺酰基，N 3或Cl。

5. 发明公开

EP0229667A3 Peptidylaminodiols 失效
标题翻译： PEPTIDYLAMINODIOLS
公开(公告)号：EP0229667A3
公开(公告)日：1991-03-13
申请号：EP87100424.8
申请日：1987-01-15
申请人： ABBOTT LABORATORIES
发明人： Luly, Jay Richard , Kempf, Dale John , Plattner, Jacob John
IPC分类号： C07K5/06 , C07K5/08 , C07K5/02 , C07D233/64 , C07C237/12 , A61K31/415 , A61K37/02 , A61K37/64 , A61K31/16
CPC分类号： C07D233/64 , A61K38/00 , C07K5/0202 , C07K5/0227 , C07K5/06026 , C07K5/06043 , C07K5/0606 , C07K5/06078 , C07K5/0806 , C07K5/0808 , C07K5/0821 , C07K5/0823 , Y02P20/55
摘要： A renin inhibiting compound of the formula:
wherein A is a substituent; W is C=O or CHOH; U is CH₂ or NR₂, provided that when W is CHOH then U is CH₂; R₁ is loweralkyl, cycloalkylmethyl, benzyl, 4-methoxybenzyl, halobenzyl, (1-naphthyl)methyl, (2-naphthyl)methyl, (4-imidazoyl)methyl, α, α -dimethylbenzyl, 1-benzyloxyethyl, phenethyl, phenoxy, thiophenoxy or anilino; R₂ is hydrogen or loweralkyl; R₃ is loweralkyl, [(alkoxy)alkoxy]alkyl, (thioalkoxy)alkyl, lowerakenyl, benzyl or heterocyclic ring substituted methyl; R₄ is loweralkyl, cycloalkylmethyl or benzyl; R₅ is vinyl, formyl, hydroxymethyl or hydrogen; R₇ is hydrogen or loweralkyl; R₈ and R₉ are independently selected from OH and NH₂; and R₆ is hydrogen, loweralkyl, vinyl or arylalkyl; provided that when R₅ and R₇ are both hydrogen and R₈ and R₉ are OH, the carbon bearing R₅ is of the "R" configuration and the carbon bearing R₆ is of the "S" configuration; or pharmaceutically acceptable salts or esters thereof. Also disclosed are renin inhibiting compositions, a method of treating hypertension, methods of making the renin inhibiting compounds and intermediates useful in making the renin inhibiting compounds.

6. 发明公开

EP0189203A3 Peptidylaminodiols 失效
公开(公告)号：EP0189203A3
公开(公告)日：1989-08-23
申请号：EP86100917.3
申请日：1986-01-23
申请人： ABBOTT LABORATORIES
发明人： Luly, Jay Richard , Plattner, John Jacob , Rosenberg, Saul Howard , Fung, Anthony K.L.
IPC分类号： C07K5/06 , C07D233/64 , A61K37/64
CPC分类号： C07K5/06078 , A61K38/00 , C07K5/0227 , C07K5/06017 , C07K5/06139 , Y02P20/55
摘要： The invention relates to renin inhibiting compounds of the formula:
wherein R 10 is
A is hydrogen or an N-protecting group; w is 0 or 1; B is hydrogen, hydroxy, NH, N-alkyl, loweralkyl or arylalkyl; with the proviso that when w is 1, B is NH and when w is 0, B is hydrogen, hydroxy, loweralkyl or arylalkyl; R 1 is loweralkyl or lipophilic or aromatic or hydrophilic amino acid side chains; m is 1-3; n is 1-3; p is 1-3; q is 1-3; s is 1-3; t is 0-2; R 2 is hydrogen or loweralkyl; R 3 and R 4 are independently selected from loweralkyl, lipophilic or aromatic amino acid side chains; R 5 and R 7 are independently selected from hydrogen or loweralkyl; and R 6 is hydrogen, loweralkyl, vinyl, arylalkyl or wherein R 8 is hydrogen or loweralkyl, X is O, NH or S and R 9 is hydrogen, loweralkyl or alkanoyl or XR 9 together can be loweralkylsulfonyl, N 3 or Cl.
摘要翻译：本发明涉及下式的肾素抑制化合物：其中R 10是A是氢或N-保护基; w是0或1; B是氢，羟基，NH，N-烷基，低级烷基或芳基烷基; 条件是当w为1时，B为NH且当w为0时，B为氢，羟基，低级烷基或芳基烷基; R1是低级烷基或亲脂性或芳族或亲水性氨基酸侧链; m是1-3; n是1-3; p是1-3; q是1-3; s是1-3; t是0-2; R2是氢或低级烷基; R3和R4独立地选自低级烷基，亲脂性或芳族氨基酸侧链; R5和R7独立地选自氢或低级烷基; 且R6为氢，低级烷基，乙烯基，芳基烷基或其中R8为氢或低级烷基，X为O，NH或S且R9为氢，低级烷基或烷酰基或XR9一起可为低级烷基磺酰基，N3或Cl。

7. 发明授权

EP0229667B1 Peptidylaminodiols 失效
公开(公告)号：EP0229667B1
公开(公告)日：1994-07-13
申请号：EP87100424.8
申请日：1987-01-15
申请人： ABBOTT LABORATORIES
发明人： Luly, Jay Richard , Kempf, Dale John , Plattner, Jacob John
IPC分类号： C07K5/06 , C07K5/08 , C07K5/02 , C07D233/64 , C07C237/12 , A61K31/415 , A61K37/02 , A61K37/64 , A61K31/16
CPC分类号： C07D233/64 , A61K38/00 , C07K5/0202 , C07K5/0227 , C07K5/06026 , C07K5/06043 , C07K5/0606 , C07K5/06078 , C07K5/0806 , C07K5/0808 , C07K5/0821 , C07K5/0823 , Y02P20/55

8. 发明公开

EP0172347A3 Renin inhibiting compounds 失效
标题翻译：雷宁抑制化合物
公开(公告)号：EP0172347A3
公开(公告)日：1989-04-05
申请号：EP85107375.9
申请日：1985-06-18
申请人： ABBOTT LABORATORIES
发明人： Luly, Jay Richard , Dellaria, Joseph F. Jr. , Plattner, John Jacob
IPC分类号： C07K5/06 , C07D233/64 , C07C103/50 , A61K37/64 , A61K31/415 , A61K31/16
CPC分类号： C07K5/06078 , A61K38/00 , C07K5/0227 , Y02P20/55 , Y10S530/86
摘要： The invention relates to renin inhibiting compounds of the formula

wherein A is an N-protecting group; n is 0 or 1; B is hydrogen, hydroxy, NH, loweralkyl or arylalkyl; with the proviso that when A is an N-protecting group, B is NH and when n is 0, B is hydrogen, hydroxy, loweralkyl or arylalkyl; R,, R 3 and R 5 are loweralkyl or hydrophilic, lipophilic or aromatic amino acid side chains and may be the same or different; R 2 , R 4 ,R 7 , R 8 and R s are hydrogen or loweralkyl and may be the same or different; X is NH, 0, S, SO or SO 2 ; and R 6 is loweralkyl, cycloalkyl, cycloalkylalkyl, aryl, arylalkyl or an N-protecting group, with the proviso that R 6 may be an N-protecting group when X is NH.
摘要翻译：本发明涉及下式的肾素抑制化合物，其中A是N-保护基; n为0或1; B是氢，羟基，NH，低级烷基或芳基烷基; 条件是当A为N-保护基团时，B为NH，当n为0时，B为氢，羟基，低级烷基或芳基烷基; R 1，R 3和R 5是低级烷基或亲水性，亲油性或芳族氨基酸侧链，可以相同或不同; R2，R4，R7，R8和R9是氢或低级烷基，可以相同或不同; X是NH，O，S，SO或SO 2; 并且R 6为低级烷基，环烷基，环烷基烷基，芳基，芳烷基或N-保护基，条件是当X为NH时，R 6可为N-保护基。

9. 发明公开

EP0172346A3 Renin inhibiting compounds 失效
标题翻译：雷宁抑制化合物
公开(公告)号：EP0172346A3
公开(公告)日：1989-02-01
申请号：EP85107374.2
申请日：1985-06-18
申请人： ABBOTT LABORATORIES
发明人： Luly, Jay Richard , Dellaria, Joseph Fred , Plattner, John Jacob
IPC分类号： C07K5/00 , C07K5/06 , C07C103/30 , C07C103/50 , A61K31/16 , A61K37/64
CPC分类号： C07K5/06078 , A61K38/00 , C07K5/0227 , Y02P20/55 , Y10S530/86
摘要： The invention relates to renin inhibiting compounds of the formula

wherein A is an N-protecting group; n is 0 or 1; B is hydrogen, hydroxy NH, loweralkyl or arylalkyl; with the proviso that when A is an N-protecting group, B is NH and when n is 0, B is hydrogen, hydroxy, loweralkyl or arylalkyl; R,, R 3 and R 5 are loweralkyl or hydrophilic, lipophilic or aromatic amino acid side chains and may be the same or different; R 2 , R 4 , R 7 , R 8 and R 9 are hydrogen or loweralkyl and may be the same or different; X is CH 2 ; R B is loweralkyl, cycloalkyl, cycloalkylalkyl, aryl or arylalkyl; and X and R 6 when taken together may be a vinylic group.
摘要翻译：本发明涉及下式的肾素抑制化合物，其中A是N-保护基; n为0或1; B是氢，羟基，NH，低级烷基或芳基烷基; 条件是当A为N-保护基团时，B为NH，当n为0时，B为氢，羟基，低级烷基或芳基烷基; R 1，R 3和R 5是低级烷基或亲水性，亲油性或芳族氨基酸侧链，可以相同或不同; R2，R4，R7，R8和R9是氢或低级烷基，可以相同或不同; X是CH 2; R6是低级烷基，环烷基，环烷基烷基，芳基或芳基烷基; 当X和R 6一起使用时可以是乙烯基。

10. 发明公开

EP0230266A2 Functionalized peptidyl aminodiols and -triols 失效
标题翻译：磷脂酰胺和三聚氰胺。
公开(公告)号：EP0230266A2
公开(公告)日：1987-07-29
申请号：EP87100422.2
申请日：1987-01-15
申请人： ABBOTT LABORATORIES
发明人： Rosenberg, Saul Howard , Plattner, Jacob John , Luly, Jay Richard
IPC分类号： C07K5/06 , C07K5/02 , C07K5/08 , C07D233/64 , A61K31/415 , A61K37/02 , A61K37/64
CPC分类号： C07D233/64 , A61K38/00 , C07K5/0227 , C07K5/06043 , C07K5/06078 , C07K5/0806
摘要： The invention relates to renin inhibiting compounds of the formula
wherein A is hydrogen; loweralkyl; arylalkyl; OR₈ or SR₈ wherein R₈ is hydrogen, loweralkyl or aminoalkyl; NR₉R₁₀ wherein R₉ and R₁₀ are independently selected from hydrogen, loweralkyl, aminoalkyl, cyanoalkyl and hydroxyalkyl;
wherein B is NH, alkylamino, S, O, CH₂ or CHOH and R₁₁ is loweralkyl, cycloalkyl, aryl, arylalkyl, alkoxy, alkenyloxy, hydroxyalkoxy, dihydroxyalkoxy, arylalkoxy, arylalkoxyalkyl, amino, alkylamino, dialkylamino, (hydroxyalkyl)(alkyl)amino, (dihydroxyalkyl)(alkyl)amino, carboxylic acid-substituted alkyl, alkoxycarbonylalkyl, aminoalkyl, N-protected aminoalkyl, alkylaminoalkyl, dialkylaminoalkyl, (N-protected) alkyl)aminoalkyl, (heterocyclic)alkyl or a substituted or unsubstituted heterocyclic; R₁ is loweralkyl, cycloalkylmethyl, benzyl, α-methylbenzyl, α, α-dimethylbenzyl, 4-methoxybenzyl, halobenzyl, (1-naphthyl)methyl, (2-naphthyl)methyl, (4-imidazoyl)methyl, phenethyl, phenoxy, thiophenoxy or anilino; provided if R₁ is phenoxy, thiophenoxy or anilino, B is CH₂ or CHOH or A is hydrogen; R₃ is loweralkyl, benzyl or heterocyclic ring-substituted methyl; R₄ is loweralkyl, cycloalkyl- methyl or benzyl; R₂, R₅ and R₆ are independently hydrogen or loweralkyl; X is O, NH or S; R₇ is hydrogen, loweralkyl, alkanoyl, alkylsulfonyl.
wherein R₁₂ and R₁₃ are independently hydrogen or loweralkyl, n is 0-2 and R₁₄ is substituted or unsubstituted penyl or heterocyclic; or XR₇ together are loweralkylsulfonyl, N₃ or Cl, and pharmaceutically acceptable salts thereof.
摘要翻译：本发明涉及式：CHEM的肾素抑制化合物，其中A是氢; 低级烷基; 芳; OR8或SR8，其中R8是氢，低级烷基或氨基烷基; NR 9 R 10，其中R 9和R 10独立地选自氢，低级烷基，氨基烷基，氰基烷基和羟烷基; 其中B是NH，烷基氨基，S，O，CH 2或CHOH，R 11是低级烷基，环烷基，芳基，芳基烷基，烷氧基，烯氧基，羟基烷氧基，二羟基烷氧基，芳基烷氧基，芳基烷氧基烷基，氨基，烷基氨基，二烷基氨基，（羟基烷基）烷基）氨基，（二羟基烷基）（烷基）氨基，羧酸取代的烷基，烷氧基羰基烷基，氨基烷基，N-保护的氨基烷基，烷基氨基烷基，二烷基氨基烷基，（N-保护的）烷基）氨基烷基，（杂环）烷基或取代或未取代的杂环 ; R1是低级烷基，环烷基甲基，苄基，α-甲基苄基，α，α-二甲基苄基，4-甲氧基苄基，卤代苄基，（1-萘基）甲基，（2-萘基）甲基，（4-咪唑基）甲基，苯乙基，苯氧基，或anilino; 如果R1是苯氧基，硫代苯氧基或苯胺基，B是CH 2或CHOH或A是氢; R3是低级烷基，苄基或杂环环取代的甲基; R4是低级烷基，环烷基 - 甲基或苄基; R2，R5和R6独立地是氢或低级烷基; X是O，NH或S; R 7是氢，低级烷基，烷酰基，烷基磺酰基。其中R 12和R 13独立地为氢或低级烷基，n为0-2，R 14为取代或未取代的吡啶基或杂环基; 或XR7一起是低级烷基磺酰基，N 3或Cl，及其药学上可接受的盐。

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