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1. 发明公开

EP0957091A1 Inhibitors of tumor necrosis factor alpha 失效
标题翻译：抑制肿瘤坏死假体α
公开(公告)号：EP0957091A1
公开(公告)日：1999-11-17
申请号：EP99200946.4
申请日：1996-08-29
申请人： CELGENE CORPORATION , Muller, George , Shire, Mary
发明人： Muller, George W. , Shire, Mary
IPC分类号： C07D209/48 , A61K31/40 , C07D209/46
CPC分类号： C07D209/48 , C07D209/46
摘要： Novel nitriles are inhibitors of tumor necrosis factor α and phosphodiesterase and can be used to combat cachexia, endotoxic shock, retrovirus replication, as asthma, and inflammatory conditions. A typical embodiment is 3-phthalimido-3-(3,4-dimethoxyphenyl) propionitrile.
摘要翻译：新型腈类是肿瘤坏死因子α和磷酸二酯酶的抑制剂，可用于抵抗恶病质，内毒素休克，逆转录病毒复制，哮喘和炎性疾病。典型的实例是3-邻苯二甲酰亚氨基-3-（3,4-二甲氧基苯基）丙腈。

2. 发明公开

EP1367051A2 Inhibitors of tumor necrosis factor alpha 失效
标题翻译：抑制肿瘤坏死假体α
公开(公告)号：EP1367051A2
公开(公告)日：2003-12-03
申请号：EP03077311.3
申请日：1996-08-29
申请人： CELGENE CORPORATION , Muller, George , Shire, Mary
发明人： Muller, George W. , Shire, Mary
IPC分类号： C07D209/48 , A61K31/40 , A61P43/00 , C07D209/46
CPC分类号： C07D209/48 , C07D209/46
摘要： Novel nitriles are inhibitors of tumor necrosis factor α and phosphodiesterase and can be used to combat cachexia, endotoxic shock, retrovirus replication, asthma, and inflammatory conditions. A typical embodiment is 3-Phthalimido-3-(3,4-dimcthoxyphenyl)propionitrile.
摘要翻译：新型腈类是肿瘤坏死因子α和磷酸二酯酶的抑制剂，可用于治疗恶病质，内毒素性休克，逆转录病毒复制，哮喘和炎性病症。典型的实施方案是3-邻苯二甲酰亚胺基-3-（3,4-二甲氧基苯基）丙腈。

3. 发明公开

EP1367051A3 Inhibitors of tumor necrosis factor alpha 失效
标题翻译：肿瘤坏死因子α抑制剂
公开(公告)号：EP1367051A3
公开(公告)日：2003-12-17
申请号：EP03077311.3
申请日：1996-08-29
申请人： CELGENE CORPORATION , Muller, George , Shire, Mary
发明人： Muller, George W. , Shire, Mary
IPC分类号： C07D209/48 , A61K31/40 , A61P43/00 , C07D209/46
CPC分类号： C07D209/48 , C07D209/46
摘要： Novel nitriles are inhibitors of tumor necrosis factor α and phosphodiesterase and can be used to combat cachexia, endotoxic shock, retrovirus replication, asthma, and inflammatory conditions. A typical embodiment is 3-Phthalimido-3-(3,4-dimcthoxyphenyl)propionitrile.

4. 发明授权

EP0957091B1 Inhibitors of tumor necrosis factor alpha 失效
标题翻译：肿瘤坏死因子α抑制剂
公开(公告)号：EP0957091B1
公开(公告)日：2003-06-04
申请号：EP99200946.4
申请日：1996-08-29
申请人： CELGENE CORPORATION , Muller, George , Shire, Mary
发明人： Muller, George W. , Shire, Mary
IPC分类号： C07D209/48 , A61K31/40 , C07D209/46
CPC分类号： C07D209/48 , C07D209/46

5. 发明授权

EP0800505B1 NOVEL IMMUNOTHERAPEUTIC ARYL AMIDES 失效
标题翻译：免疫抑制剂ARYLAMIDE
公开(公告)号：EP0800505B1
公开(公告)日：2001-09-26
申请号：EP95941438.4
申请日：1995-11-20
申请人： CELGENE CORPORATION , Muller, George , Shire, Mary , Stirling, David J.
发明人： Muller, George , Shire, Mary , Stirling, David, I.
IPC分类号： C07C233/87 , C07C237/36 , C07D213/82 , A61K31/215 , A61K31/455
CPC分类号： C07D213/82 , A61K31/165 , A61K31/166 , A61K31/216 , A61K31/455 , C07C233/47 , C07C233/84 , C07C233/87 , C07C235/52 , C07C237/36 , C07C2601/14 , Y02A50/411
摘要： Novel aryl amides are inhibitors of tumor necrosis factor alpha and can be used to combat cachexia, endotoxic shock, and retrovirus replication. A typical embodiment is N-benzoyl-3-amino-3-(3',4'-dimethoxyphenyl)propanamide.
摘要翻译：新型芳基酰胺是肿瘤坏死因子α的抑制剂，可用于抵抗恶病质，内毒素性休克和逆转录病毒复制。典型的实施方案是N-苯甲酰基-3-氨基-3-（3'，4'-二甲氧基苯基）丙酰胺。

6. 发明授权

EP1468991B1 Imides as PDE III, PDE IV and TNF inhibitors 失效
标题翻译：酰亚胺作为PDE III，PDE IV和TNF抑制剂
公开(公告)号：EP1468991B1
公开(公告)日：2008-02-20
申请号：EP04076505.9
申请日：1996-12-24
申请人： CELGENE CORPORATION
发明人： Muller, George W. , Shire, Mary
IPC分类号： C07D209/48 , C07D209/46 , A61K31/40 , A61P29/00 , A61P31/00 , A61P35/00
CPC分类号： C07D209/48 , C07D209/46

7. 发明公开

EP1361210A3 Novel immunotherapeutic agents and their use in the reduction of cytokine levels 失效
标题翻译：新的免疫治疗剂及其在降低细胞因子水平中的用途
公开(公告)号：EP1361210A3
公开(公告)日：2003-11-19
申请号：EP03002806.2
申请日：1997-08-11
申请人： CELGENE CORPORATION
发明人： Muller, George W. , Shire, Mary
IPC分类号： C07C255/37 , C07C235/32 , C07C69/612 , C07C62/10 , C07C49/175 , A61K31/275 , A61K31/215 , A61K31/19 , A61K31/16 , A61K31/12 , C07C43/215 , C07C43/235 , C07C43/243 , C07C45/00 , C07C45/46 , C07C45/69 , C07C49/255 , C07C69/734 , C07C205/45 , C07C235/34 , C07D213/57 , C07D307/54 , C07D317/60
CPC分类号： C07D317/60 , C07C43/215 , C07C43/235 , C07C43/243 , C07C45/00 , C07C45/46 , C07C45/69 , C07C49/255 , C07C67/343 , C07C69/734 , C07C205/45 , C07C225/22 , C07C235/34 , C07C255/34 , C07C255/37 , C07C2601/08 , C07D213/57 , C07D307/54 , C07C49/84 , C07C49/784 , C07C69/616
摘要： Cyano and carboxy derivatives of substituted styrenes of formula I (a) X is -(CnH2n)- in which n has a value of 1, 2 or 3, and R1 is alkyl of 1 to 10 carbon atoms, monocycloaIkyl of up to 10 carbon atoms, polycycloalkyl of up to 10 carbon atoms, or benzocyclic alkyl of up to 10 carbon atoms, or (b) X is -CH= and R1 is alkylidene of up to 10 carbon atoms, monocycloalkylidene of up to 10 carbon atoms, or bicycloalkylidene of up to 10 carbon atoms; R 2 is hydrogen, nitro, cyano, trifluoromethyl, carbethoxy, carbomethoxy, carbopropoxy, acetyl, carbamoyl, acetoxy, carboxy, hydroxy, amino, alkyl of 1 to 6 carbon atoms, alkylidenemethyl of 1 to 6 carbon atoms, alkoxy of 1 to 6 carbon atoms, or halo; and R 3 is ( i ) phenyl, unsubstituted or substituted with I or more substituents each selected independently from nitro, cyano, halo, trifluoromethyl, carbethoxy, carbomethoxy, carbopropoxy, acetyl, carbamoyl, or carbamoyl substituted with alkyl of 1 to 3 carbon atoms, acetoxy, carboxy, hydroxy, amino, amino substituted with an alkyl of 1 to 5 carbon atoms, alkyl of up to 10 carbon atoms, cycloalkyl of up to 10 carbon atoms, alkoxy of up to 10 carbon atoms, cycloalkoxy of up to 10 carbon atoms, alkylidenemethyl of up to 10 carbon atoms, cycloalkylidenemethyl of up to 10 carbon atoms, phenyl, or methylenedioxy; ( ii ) pyridine, substituted pyridine, pyrrolidine, imidizole, naphthalene, or thiophene; ( iii ) cycloalkyl of 4 -10 carbon atoms, unsubstituted or substituted with 1 or more substituents each selected independently from the group consisting of nitro, cyano, halo, trifluoromethyl, carbethoxy, carbomethoxy, carbopropoxy, acetyl, carbamoyl, acetoxy, carboxy, hydroxy, amino, substituted amino, alkyl of 1 to 10 carbon atoms, alkoxy of 1 to 10 carbon atoms, phenyl; each of R 4 and R 5 taken individually is hydrogen or R 4 and R 5 taken together are a carbon-carbon bond; Y is -C≡ N, or when R 4 and R 5 are hydrogen, Y is alternatively -COZ with the provisos that; (iv) when Y is -COZ, Z is -NHR6R6 and R6 is hydrogen, then R1 is not methyl; (v) when Y is -COZ, Z is -OH or -OR7 and R7 is benzyl, then R1 is not methyl; and (vi) when Y is -COZ and Z is R7 benzyl, then R1 is not methyl and R3 is hydroxy substituted phenyl. Z is -OH, -NR 6 R 6 , R 7 or OR 7 ; R 6 is hydrogen or alkyl of 1 to 6 carbon atoms; and R 7 is alkyl or benzyl; are inhibitors of tumor necrosis factor α, and nuclear factor kB and phosphodiesterase and can be used to combat cachexia, endotoxic shock, retrovirus replication, asthma, and inflammatory conditions.
摘要翻译：式（a）的取代苯乙烯的氰基和羧基衍生物X是 - （C n H 2n） - 其中n的值为1,2或3，并且R 1为1-10个碳原子的烷基，最多10个碳的单环烷基原子，多达10个碳原子的多环烷基或多达10个碳原子的苯并环烷基，或（b）X是-CH =并且R 1是至多10个碳原子的亚烷基，最多10个碳原子的亚环烷基或二亚环烷基多达10个碳原子; R2为氢，硝基，氰基，三氟甲基，乙氧基羰基，甲氧甲酰基，丙氧羰基，乙酰基，氨基甲酰基，乙酰氧基，羧基，羟基，氨基，1-6个碳原子的烷基，1-6个碳原子的亚烷基甲基，1-6个碳原子的烷氧基原子或光环; （i）未被取代或被1个或多个独立选自硝基，氰基，卤素，三氟甲基，乙氧基羰基，甲氧基羰基，丙氧基羰基，乙酰基，氨基甲酰基或被1-3个碳原子的烷基取代的氨基甲酰基取代的取代基取代的苯基，乙酰氧基，羧基，羟基，氨基，被1-5个碳原子的烷基取代的氨基，最多10个碳原子的烷基，最多10个碳原子的环烷基，最多10个碳原子的烷氧基，最多10个碳的环烷氧基原子，最多10个碳原子的亚烷基甲基，最多10个碳原子的亚环烷基甲基，苯基或亚甲二氧基; （ii）吡啶，取代的吡啶，吡咯烷，咪唑，萘或噻吩; （iii）未取代的或被1个或多个独立选自硝基，氰基，卤素，三氟甲基，乙氧羰基，甲氧甲酰基，丙氧羰基，乙酰基，氨基甲酰基，乙酰氧基，羧基，羟基，氨基，取代的氨基，1至10个碳原子的烷基，1至10个碳原子的烷氧基，苯基; R4和R5各自独立地为氢或者R4和R5一起为碳 - 碳键; Y是-C≡N，或者当R4和R5是氢时，Y或者是-COZ，条件是：（iv）当Y是-COZ时，Z是-NHR6R6并且R6是氢，则R1不是甲基; （v）当Y是-COZ时，Z是-OH或-OR 7且R 7是苄基，则R 1不是甲基; 和（vi）当Y是-COZ且Z是R7苄基时，则R1不是甲基且R3是羟基取代的苯基。 Z是-OH，-NR 6 R 6，R 7或OR 7; R6是氢或1至6个碳原子的烷基; 和R7是烷基或苄基; 是肿瘤坏死因子α和核因子κB和磷酸二酯酶的抑制剂，并且可用于对抗恶病质，内毒素休克，逆转录病毒复制，哮喘和炎性病症。

8. 发明授权

EP1361210B1 Novel immunotherapeutic agents and their use in the reduction of cytokine levels 失效
标题翻译：新的免疫治疗剂及其在减少Cytokinenspiegel使用
公开(公告)号：EP1361210B1
公开(公告)日：2008-12-24
申请号：EP03002806.2
申请日：1997-08-11
申请人： CELGENE CORPORATION
发明人： Muller, George W. , Shire, Mary
IPC分类号： C07C255/37 , C07C235/32 , A61K31/275
CPC分类号： C07D317/60 , C07C43/215 , C07C43/235 , C07C43/243 , C07C45/00 , C07C45/46 , C07C45/69 , C07C49/255 , C07C67/343 , C07C69/734 , C07C205/45 , C07C225/22 , C07C235/34 , C07C255/34 , C07C255/37 , C07C2601/08 , C07D213/57 , C07D307/54 , C07C49/84 , C07C49/784 , C07C69/616

9. 发明公开

EP1468991A1 Imides as PDE III, PDE IV and TNF inhibitors 失效
标题翻译： Imide als PDE III，PDE IV和TNF Inhibitoren
公开(公告)号：EP1468991A1
公开(公告)日：2004-10-20
申请号：EP04076505.9
申请日：1996-12-24
申请人： CELGENE CORPORATION
发明人： Muller, George W. , Shire, Mary
IPC分类号： C07D209/48 , C07D209/46 , A61K31/40 , A61P29/00 , A61P31/00 , A61P35/00
CPC分类号： C07D209/48 , C07D209/46
摘要： 1. Use of a compound of the formula
in which:

one of R 1 and R 2 is R 3 -X and the other is hydrogen, nitro, cyano, trifluoromethyl, carbo(lower)alkoxy, acetyl, carbamoyl, acetoxy, carboxy, hydroxy, amino, lower alkyl, alkylamino, lower alkoxy, halo, HF 2 CO, F 3 CO or R 3 -X-;
R 3 is monocycloalkyl, bicycloalkyl or benzocycloalkyl of up to 18 carbon atoms, tetrahydropyran or tetrahydrofuran;
X is a carbon-carbon bond, -CH 2 -, -O- or -N=;
R 5 is (i) o-phenylene, unsubstituted or substituted with 1 or more substituents each selected independently from nitro, cyano, halo, trifluoromethyl, carbo(lower)alkoxy, acetyl, or carbamoyl, unsubstituted or substituted with lower alkyl, acetoxy, carboxy, hydroxy, amino, lower alkylamino, lower acylamino, aminoalkyl, or lower alkoxy; (ii) the vicinally divalent residue of pyridine, pyrrolidine, imidizole, naphthalene, or thiophene, wherein the divalent bonds are on vicinal ring carbon atoms; (iii) a vicinally divalent cycloalkyl or cycloalkenyl of 4-10 carbon atoms, unsubstituted or substituted with one or more substituents each selected independently from the group consisting of nitro, cyano, halo, trifluoromethyl, carbo(lower)alkoxy, acetyl, carbamoyl, acetoxy, carboxy, hydroxy, amino, lower alkylamino, lower alkyl, lower alkoxy, or phenyl; (iv) vinylene di-substituted with lower alkyl; or (v) ethylene, unsubstituted or monosubstituted or disubstituted with lower alkyl;
R 6 is -CO-, -CH 2 - or -CH 2 CO-;
Y is -COZ, -CN, -OR 8 , lower alkyl or aryl,
Z is -NH 2 , -OH, -NHR, -R 9 , or -OR 9 ;
R 8 is hydrogen or lower alkyl;
R 9 is lower alkyl or benzyl, and
n has a value of 0, 1, 2, or 3,
wherein the term "lower" denotes from 1 to 6 carbon atoms, for the manufacture of a medicament for treating cancer.
摘要翻译： 1.式化合物的用途，其中：R 1和R 2之一为R 3 -X，另一个为氢，硝基，氰基，三氟甲基，碳（低级）烷氧基，乙酰基，氨基甲酰基，乙酰氧基，羧基，羟基，氨基，低级烷基，烷基氨基，低级烷氧基，卤素，HF 2 CO，F 3 CO或R 3 -X-; R 3是具有至多18个碳原子的单环烷基，双环烷基或苯并环烷基，四氢吡喃或四氢呋喃; X是碳 - 碳键，-CH 2 - ， - O-或-N = 氰基，卤素，三氟甲基，碳（低级）烷氧基，乙酰基或氨基甲酰基，未取代或被低级烷基取代的（I）o-亚苯基，未取代或被1个或多个取代基取代，乙酰氧基，羧基，羟基，氨基，低级烷基氨基，低级酰基氨基，氨基烷基或低级烷氧基; （ii）吡啶，吡咯烷，亚胺唑，萘或噻吩的相邻二价残基，其中二价键位于连环碳原子上; （iii）4-10个碳原子的邻位二价环烷基或环烯基，未取代或被一个或多个取代基取代，各自独立地选自硝基，氰基，卤素，三氟甲基，碳（低级）烷氧基，乙酰基，氨基甲酰基，乙酰氧基，羧基，羟基，氨基，低级烷基氨基，低级烷基，低级烷氧基或苯基; （iv）用低级烷基二取代的亚乙烯基; 或（v）乙烯，未被取代或被低级烷基单取代或双取代; R 6是-CO - ， - CH 2 - 或-CH 2 CO-; Y是-COZ，-CN，-OR 8，低级烷基或芳基，Z是-NH 2，-OH，-NHR，-R 9或-OR 9。 R 8是氢或低级烷基; R 9为低级烷基或苄基，n为0,1,2或3，其中术语“低级”表示1至6个碳原子，用于制备用于治疗癌症的药物。

10. 发明公开

EP1361210A2 Novel immunotherapeutic agents and their use in the reduction of cytokine levels 失效
标题翻译： Neue immunotherapeutische Mittel und deren Verwendung in der Reduzierung von Cytokinenspiegel
公开(公告)号：EP1361210A2
公开(公告)日：2003-11-12
申请号：EP03002806.2
申请日：1997-08-11
申请人： CELGENE CORPORATION
发明人： Muller, George W. , Shire, Mary
IPC分类号： C07C255/37 , C07C235/32 , C07C69/612 , C07C62/10 , C07C49/175 , A61K31/275 , A61K31/215 , A61K31/19 , A61K31/16 , A61K31/12 , C07C43/215 , C07C43/235 , C07C43/243 , C07C45/00 , C07C45/46 , C07C45/69 , C07C49/255 , C07C69/734 , C07C205/45 , C07C235/34 , C07D213/57 , C07D307/54 , C07D317/60
CPC分类号： C07D317/60 , C07C43/215 , C07C43/235 , C07C43/243 , C07C45/00 , C07C45/46 , C07C45/69 , C07C49/255 , C07C67/343 , C07C69/734 , C07C205/45 , C07C225/22 , C07C235/34 , C07C255/34 , C07C255/37 , C07C2601/08 , C07D213/57 , C07D307/54 , C07C49/84 , C07C49/784 , C07C69/616
摘要： Cyano and carboxy derivatives of substituted styrenes of formula I

(a) X is -(C n H 2n )- in which n has a value of 1, 2 or 3, and R 1 is alkyl of 1 to 10 carbon atoms, monocycloaIkyl of up to 10 carbon atoms, polycycloalkyl of up to 10 carbon atoms, or benzocyclic alkyl of up to 10 carbon atoms, or
(b) X is -CH= and R 1 is alkylidene of up to 10 carbon atoms, monocycloalkylidene of up to 10 carbon atoms, or bicycloalkylidene of up to 10 carbon atoms;

R 2 is hydrogen, nitro, cyano, trifluoromethyl, carbethoxy, carbomethoxy, carbopropoxy, acetyl, carbamoyl, acetoxy, carboxy, hydroxy, amino, alkyl of 1 to 6 carbon atoms, alkylidenemethyl of 1 to 6 carbon atoms, alkoxy of 1 to 6 carbon atoms, or halo; and
R 3 is ( i ) phenyl, unsubstituted or substituted with I or more substituents each selected independently from nitro, cyano, halo, trifluoromethyl, carbethoxy, carbomethoxy, carbopropoxy, acetyl, carbamoyl, or carbamoyl substituted with alkyl of 1 to 3 carbon atoms, acetoxy, carboxy, hydroxy, amino, amino substituted with an alkyl of 1 to 5 carbon atoms, alkyl of up to 10 carbon atoms, cycloalkyl of up to 10 carbon atoms, alkoxy of up to 10 carbon atoms, cycloalkoxy of up to 10 carbon atoms, alkylidenemethyl of up to 10 carbon atoms, cycloalkylidenemethyl of up to 10 carbon atoms, phenyl, or methylenedioxy; ( ii ) pyridine, substituted pyridine, pyrrolidine, imidizole, naphthalene, or thiophene; ( iii ) cycloalkyl of 4 -10 carbon atoms, unsubstituted or substituted with 1 or more substituents each selected independently from the group consisting of nitro, cyano, halo, trifluoromethyl, carbethoxy, carbomethoxy, carbopropoxy, acetyl, carbamoyl, acetoxy, carboxy, hydroxy, amino, substituted amino, alkyl of 1 to 10 carbon atoms, alkoxy of 1 to 10 carbon atoms, phenyl;
each of R 4 and R 5 taken individually is hydrogen or R 4 and R 5 taken together are a carbon-carbon bond;

Y is -C≡ N, or when R 4 and R 5 are hydrogen, Y is alternatively -COZ with the provisos that;

(iv) when Y is -COZ, Z is -NHR 6 R 6 and R 6 is hydrogen, then R 1 is not methyl;
(v) when Y is -COZ, Z is -OH or -OR 7 and R 7 is benzyl, then R 1 is not methyl; and
(vi) when Y is -COZ and Z is R 7 benzyl, then R 1 is not methyl and R 3 is hydroxy substituted phenyl.
Z is -OH, -NR 6 R 6 , R 7 or OR 7 ;

R 6 is hydrogen or alkyl of 1 to 6 carbon atoms; and
R 7 is alkyl or benzyl; are inhibitors of tumor necrosis factor α, and nuclear factor kB and phosphodiesterase and can be used to combat cachexia, endotoxic shock, retrovirus replication, asthma, and inflammatory conditions.
摘要翻译：式（I）的取代苯乙烯的氰基和羧基衍生物（a）X是 - （C n H 2n） - 其中n具有1,2或3的数值，并且R 1是1至10个碳原子的烷基，最多10个碳原子的单环烷基，至多10个碳原子的多环烷基或至多10个碳原子的苯并环烷基，或（b）X是-CH =和R 1是至多10个碳原子的亚烷基，单环亚烷基至多10个碳原子，或至多10个碳原子的双亚烷基; R 2是氢，硝基，氰基，三氟甲基，乙酯基，甲酯基，碳丙氧基，乙酰基，氨基甲酰基，乙酰氧基，羧基，羟基，氨基，1至6个碳原子的烷基，1至6个碳原子的亚烷基甲基，至6个碳原子，或卤素; 氰基，卤素，三氟甲基，乙氧羰基，甲酯基，碳丙氧基，乙酰基，氨基甲酰基或被1至3个烷基取代的氨基甲酰基取代的取代或未取代的苯基，碳原子，乙酰氧基，羧基，羟基，氨基，被1至5个碳原子的烷基取代的氨基，至多10个碳原子的烷基，至多10个碳原子的烷基，至多10个碳原子的烷氧基，至多10个碳原子的亚烷基甲基，至多10个碳原子的亚环烷基甲基，苯基或亚甲二氧基; （ii）吡啶，取代的吡啶，吡咯烷，亚胺唑，萘或噻吩; （iii）4至10个碳原子的环烷基，未取代或被1个或多个取代基取代，各自独立地选自硝基，氰基，卤素，三氟甲基，乙氧基，甲酯基，碳丙氧基，乙酰基，氨基甲酰基，乙酰氧基，羧基，羟基，氨基，取代的氨基，1至10个碳原子的烷基，1至10个碳原子的烷氧基，苯基; 单独取代的R 4和R 5各自为氢或R 4和R 5一起为碳 - 碳键; Y为-C定义N，或当R 4和R 5为氢时，Y为-COZ，条件是：（iv）当Y为-COZ时，Z为-NHR 6 R 6且R 6为氢，则R 1不为甲基; （ⅴ）当Y为-COZ时，Z为-OH或-OR 7，R 7为苄基，则R 1不为甲基; 和（vi）当Y是-COZ且Z是R 7苄基时，R 1不是甲基，R 3是羟基取代的苯基。 Z是-OH，-NR 6 R 6，R 7或OR 7; R 6是氢或1至6个碳原子的烷基; 和R 7是烷基或苄基; 是肿瘤坏死因子α和核因子kB和磷酸二酯酶的抑制剂，可用于治疗恶病质，内毒素性休克，逆转录病毒复制，哮喘和炎性病症。式I的取代苯乙烯的酰基和羧基衍生物（a） X为 - （C n H 2n） - 其中n为1,2或3，R 1为1至10个碳原子的烷基，至多10个碳原子的单环烷基，至多10个碳原子的多环烷基，或至多10个碳原子的苯并环烷基，或（b）X为-CH =且R 1为至多10个碳原子的亚烷基，至多10个碳原子的单环亚烷基或至多10个碳原子的双亚烷基; R 2是氢，硝基，氰基，三氟甲基，乙酯基，甲酯基，碳丙氧基，乙酰基，氨基甲酰基，乙酰氧基，羧基，羟基，氨基，1至6个碳原子的烷基，1至6个碳原子的亚烷基甲基，至6个碳原子，或卤素; 氰基，卤素，三氟甲基，乙氧羰基，甲酯基，碳丙氧基，乙酰基，氨基甲酰基或被1至3个烷基取代的氨基甲酰基取代的取代或未取代的苯基，碳原子，乙酰氧基，羧基，羟基，氨基，被1至5个碳原子的烷基取代的氨基，至多10个碳原子的烷基，至多10个碳原子的烷基，至多10个碳原子的烷氧基，至多10个碳原子的亚烷基甲基，至多10个碳原子的亚环烷基甲基，苯基或亚甲二氧基; （ii）吡啶，取代的吡啶，吡咯烷，亚胺唑，萘或噻吩; （iii）环烷基

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