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公开(公告)号：US20060040869A1
公开(公告)日：2006-02-23
申请号：US11059086
申请日：2005-02-07
IPC分类号： A61K38/05 , A61K38/04 , A61K31/198 , C07C323/39 , C07K5/04 , C07K5/06
CPC分类号： C07C323/59 , C07C45/673 , C07C49/647 , C07C49/653 , C07C49/657 , C07C49/753 , C07C205/45 , C07C225/20 , C07C233/32 , C07C233/76 , C07C271/24 , C07C271/36 , C07C271/56 , C07C271/66 , C07C311/20 , C07C311/53 , C07C323/43 , C07C2601/08 , C07C2601/10
摘要： A compound of formula (I) or (II): wherein A is hydrogen or CR1R2; Y and Z are each, independently, hydrogen or a halogen; X is —NR4R5, or R7; R1 is hydrogen, or a substituted or unsubstituted alkyl or alkenyl group containing 1-4 carbon atoms; when X is —NR4R5, R2 is a substituted or unsubstituted alkyl, alkenyl, alkynyl, aryl, aralkyl aralkenyl, or aralkynyl group, that optionally includes at least one heteroatom in its carbon skeleton and contains 1-12 carbon atoms; when X is R7, R2 is an unsubstituted alkyl, alkenyl or alkynyl group, or a substituted or unsubstituted aryl, aralkyl aralkenyl, or aralkynyl group, that optionally includes at least one heteroatom in its carbon skeleton and contains 1-12 carbon atoms; R3 is a substituted or unsubstituted alkyl, alkenyl, alkynyl, aryl, aralkyl aralkenyl, or aralkynyl group, that optionally includes at least one heteroatom in its carbon skeleton and contains 1-12 carbon atoms; R4 is hydrogen, a substituted or unsubstituted alkyl, alkenyl, alkynyl, aryl, aralkyl aralkenyl, or aralkynyl group, that optionally includes at least one heteroatom in its carbon skeleton and contains 1-12 carbon atoms, —COOR8, or —COR8; R5 is hydrogen, or a substituted or unsubstituted alkyl or alkenyl group containing 1-5 carbon atoms; R7 is an unsubstituted alkyl, alkenyl, or alkynyl group, that contains 1-4 carbon atoms; and, R8 is an unsubstituted or halo-substituted alkyl, aryl, or aralkyl group, that contains 1-12 carbon atoms.
摘要翻译： 式（I）或（II）的化合物：其中A是氢或CR 1 R 2; Y和Z各自独立地为氢或卤素; X是-NR 4 R 5或R 7; R 1是氢或含有1-4个碳原子的取代或未取代的烷基或链烯基; 当X是-NR 4 R 5时，R 2是取代或未取代的烷基，烯基，炔基，芳基，芳烷基芳烯基或芳炔基 基团，其任选地在其碳骨架中包含至少一个杂原子并且含有1-12个碳原子; 当X是R 7时，R 2是未取代的烷基，烯基或炔基，或取代或未取代的芳基，芳烷基芳烯基或芳炔基，其任选地包括在 其碳骨架中至少有一个杂原子，含有1-12个碳原子; R 3是取代或未取代的烷基，烯基，炔基，芳基，芳烷基芳烯基或芳炔基，其任选地在其碳骨架中包含至少一个杂原子并含有1-12个碳原子; R 4是氢，取代或未取代的烷基，烯基，炔基，芳基，芳烷基芳烯基或芳炔基，其任选地在其碳骨架中包含至少一个杂原子并含有1-12个碳原子， -COOR 8或-COR 8; R 5是氢或含有1-5个碳原子的取代或未取代的烷基或链烯基; R 7是含有1-4个碳原子的未取代的烷基，烯基或炔基; R 8是含有1-12个碳原子的未取代或卤素取代的烷基，芳基或芳烷基。
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公开(公告)号：US20060252839A1
公开(公告)日：2006-11-09
申请号：US10957242
申请日：2004-09-27
申请人： Stanley Roberts , Maria Gabriella Santoro , Vasudev Jadhav , Alan Happe , Paul Evans , Nicolette Ross , Timothy Snape
发明人： Stanley Roberts , Maria Gabriella Santoro , Vasudev Jadhav , Alan Happe , Paul Evans , Nicolette Ross , Timothy Snape
IPC分类号： A61K31/10 , C07C323/22
CPC分类号： C07C323/22 , C07C323/59 , C07C2601/08 , C07C2601/10 , C07F7/1804
摘要： A compound comprising a cyclopentanone, cyclopentenone, cyclohexanone or cyclohexenone group, wherein a first ring carbon atom carries an —SR substituent, R is a substituted or unsubstituted alkyl, alkenyl, alkynyl, aryl, aralkyl, aralkenyl, or aralkynyl group that, optionally, includes at least one heteroatom in its carbon skeleton, the remaining available ring carbon atoms are optionally substituted, and said compound either:—(a) is more soluble in water at a temperature of 20-40° C.; (b) is less lipophilic; and/or, (c) has a greater therapeutic index; or; (d) is less soluble in water at a temperature of 20-40° C.; (e) is more lipophilic; and/or, (f) has a greater therapeutic index; than an equivalent cyclohex-2-en-1-one or cyclopent-2-en-1-one derivative in which a hydrogen atom replaces said —SR group.
摘要翻译： 包含环戊酮，环戊烯酮，环己酮或环己烯酮基团的化合物，其中第一环碳原子带有-SR取代基，R是取代或未取代的烷基，烯基，炔基，芳基，芳烷基，芳烯基或芳炔基， 在其碳骨架中包含至少一个杂原子，剩余的可用环碳原子任选被取代，并且所述化合物： - （a）在20-40℃的温度下更易溶于水; （b）亲脂性较差; 和/或（c）具有较大的治疗指数; 要么; （d）在20-40℃的温度下较少溶于水; （e）更亲脂; 和/或（f）具有较大的治疗指数; 比其中氢原子取代所述-SR基团的当量环己-2-烯-1-酮或环戊-2-烯-1-酮衍生物。
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公开(公告)号：US07759399B2
公开(公告)日：2010-07-20
申请号：US10957242
申请日：2004-09-27
申请人： Stanley Michael Roberts , Maria Gabriella Santoro , Vasudev Jadhav , Alan Michael Happe , Paul Evans , Nicolette Christa Ross , Timothy James Snape
发明人： Stanley Michael Roberts , Maria Gabriella Santoro , Vasudev Jadhav , Alan Michael Happe , Paul Evans , Nicolette Christa Ross , Timothy James Snape
IPC分类号： A01N31/00
CPC分类号： C07C323/22 , C07C323/59 , C07C2601/08 , C07C2601/10 , C07F7/1804
摘要： A compound comprising a cyclopentanone, cyclopentenone, cyclohexanone or cyclohexenone group, wherein a first ring carbon atom carries an —SR substituent, R is a substituted or unsubstituted alkyl, alkenyl, alkynyl, aryl, aralkyl, aralkenyl, or aralkynyl group that, optionally, includes at least one heteroatom in its carbon skeleton, the remaining available ring carbon atoms are optionally substituted, and said compound either: —(a) is more soluble in water at a temperature of 20-40° C.; (b) is less lipophilic; and/or, (c) has a greater therapeutic index; or; (d) is less soluble in water at a temperature of 20-40° C.; (e) is more lipophilic; and/or, (f) has a greater therapeutic index; than an equivalent cyclohex-2-en-1-one or cyclopent-2-en-1-one derivative in which a hydrogen atom replaces said —SR group.
摘要翻译： 包含环戊酮，环戊烯酮，环己酮或环己烯酮基团的化合物，其中第一环碳原子带有-SR取代基，R是取代或未取代的烷基，烯基，炔基，芳基，芳烷基，芳烯基或芳炔基， 在其碳骨架中包含至少一个杂原子，剩余的可用环碳原子任选被取代，并且所述化合物： - （a）在20-40℃的温度下更可溶于水; （b）亲脂性较差; 和/或（c）具有较大的治疗指数; 要么; （d）在20-40℃的温度下较少溶于水; （e）更亲脂; 和/或（f）具有较大的治疗指数; 比其中氢原子取代所述-SR基团的当量环己-2-烯-1-酮或环戊-2-烯-1-酮衍生物。
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公开(公告)号：US07183440B2
公开(公告)日：2007-02-27
申请号：US11059086
申请日：2005-02-07
申请人： Stanley Michael Roberts , Maria Gabriella Santoro , Vasudev Jadhav , Alan Michael Happe , Jérôme Dauvergne
发明人： Stanley Michael Roberts , Maria Gabriella Santoro , Vasudev Jadhav , Alan Michael Happe , Jérôme Dauvergne
IPC分类号： C07C315/00 , C07C49/00 , A61K31/12 , A61K31/095
CPC分类号： C07C323/59 , C07C45/673 , C07C49/647 , C07C49/653 , C07C49/657 , C07C49/753 , C07C205/45 , C07C225/20 , C07C233/32 , C07C233/76 , C07C271/24 , C07C271/36 , C07C271/56 , C07C271/66 , C07C311/20 , C07C311/53 , C07C323/43 , C07C2601/08 , C07C2601/10
摘要： A compound of formula (I) or (II): wherein A is hydrogen or CR1R2; Y and Z are each, independently, hydrogen or a halogen; X is —NR4R5, or R7; R1 is hydrogen, or a substituted or unsubstituted alkyl or alkenyl group containing 1–4 carbon atoms; when X is —NR4R5, R2 is a substituted or unsubstituted alkyl, alkenyl, alkynyl, aryl, aralkyl aralkenyl, or aralkynyl group, that optionally includes at least one heteroatom in its carbon skeleton and contains 1–12 carbon atoms; when X is R7, R2 is an unsubstituted alkyl, alkenyl or alkynyl group, or a substituted or unsubstituted aryl, aralkyl aralkenyl, or aralkynyl group, that optionally includes at least one heteroatom in its carbon skeleton and contains 1–12 carbon atoms; R3 is a substituted or unsubstituted alkyl, alkenyl, alkynyl, aryl, aralkyl aralkenyl, or aralkynyl group, that optionally includes at least one heteroatom in its carbon skeleton and contains 1–12 carbon atoms; R4 is hydrogen, a substituted or unsubstituted alkyl, alkenyl, alkynyl, aryl, aralkyl aralkenyl, or aralkynyl group, that optionally includes at least one heteroatom in its carbon skeleton and contains 1–12 carbon atoms, —COOR8, or —COR8; R5 is hydrogen, or a substituted or unsubstituted alkyl or alkenyl group containing 1–5 carbon atoms; R7 is an unsubstituted alkyl, alkenyl, or alkynyl group, that contains 1–4 carbon atoms; and, R8 is an unsubstituted or halo-substituted alkyl, aryl, or aralkyl group, that contains 1–12 carbon atoms
摘要翻译： 式（I）或（II）的化合物：其中A是氢或CR 1 R 2; Y和Z各自独立地为氢或卤素; X是-NR 4 R 5或R 7; R 1是氢或含有1-4个碳原子的取代或未取代的烷基或链烯基; 当X是-NR 4 R 5时，R 2是取代或未取代的烷基，烯基，炔基，芳基，芳烷基芳烯基或芳炔基 基团，其任选地在其碳骨架中包含至少一个杂原子并且含有1-12个碳原子; 当X是R 7时，R 2是未取代的烷基，烯基或炔基，或取代或未取代的芳基，芳烷基芳烯基或芳炔基，其任选地包括在 其碳骨架中至少有一个杂原子，含有1-12个碳原子; R 3是取代或未取代的烷基，烯基，炔基，芳基，芳烷基芳烯基或芳炔基，其任选地在其碳骨架中包含至少一个杂原子并含有1-12个碳原子; R 4是氢，取代或未取代的烷基，烯基，炔基，芳基，芳烷基芳烯基或芳炔基，其任选地在其碳骨架中包含至少一个杂原子并含有1-12个碳原子， -COOR 8或-COR 8; R 5是氢或含有1-5个碳原子的取代或未取代的烷基或链烯基; R 7是含有1-4个碳原子的未取代的烷基，烯基或炔基; 并且R 8是含有1-12个碳原子的未取代或卤素取代的烷基，芳基或芳烷基
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公开(公告)号：US06180681B2
公开(公告)日：2001-01-30
申请号：US09202553
申请日：1998-12-16
IPC分类号： A61K3112
CPC分类号： A61K31/122
摘要： The invention relates to 2-cyclopenten-1-one as an inducer of the heat shock protein HSP70 by activating the heat shock transcription factor HSF, and selectively inducing the transcription and translation of HSP70 in human cells. In particular, since a cytoprotective role of HSP70 during viral infection was previously shown, the invention refers to 2-cyclopenten-1-one and its pharmaceutically acceptable derivatives as inducers of HSP70 with antiviral activity. Treatment with 2-cyclopenten-1-one and its pharmaceutically acceptable derivatives causes a dose-dependent reduction of infectious virus yield during infection with vesicular stomatitis virus. The block of virus replication is due to inhibition of viral protein synthesis, associated with HSP70 synthesis.
摘要翻译： 本发明涉及2-环戊烯-1-酮作为热休克蛋白HSP70的诱导剂，通过激活热休克转录因子HSF，并选择性诱导人细胞中HSP70的转录和翻译。 特别地，由于先前已显示出病毒感染期间HSP70的细胞保护作用，所以本发明涉及2-环戊烯-1-酮及其药学上可接受的衍生物作为具有抗病毒活性的HSP70诱导剂。 用2-环戊烯-1-酮及其药学上可接受的衍生物的治疗导致在水泡性口炎病毒感染期间感染性病毒产量的剂量依赖性降低。 病毒复制的阻断是由于与HSP70合成相关的病毒蛋白合成的抑制。
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6.发明授权2-cyclopenten-1-one and its derivatives as inhibitors of the NF-kB factor 失效2-环戊烯-1-酮及其衍生物作为NF-kB因子的抑制剂公开(公告)号：US06696498B2
公开(公告)日：2004-02-24
申请号：US10142813
申请日：2002-05-10
IPC分类号： A01N3500
CPC分类号： A61K31/122 , A61K31/42 , A61K2300/00
摘要： 2-Cyclopenten-1-one and its derivatives comprising the cyclopentenone nucleus as inhibitors of the NF-kB factor, with anti-inflammatory, anti-proliferative-immuno-suppressive, cytoprotective and antiviral activity, the substituents being selected among the ones which do not affect NF-kB inhibitory activity.
摘要翻译： 包含环戊烯酮核的2-环戊烯-1-酮及其衍生物作为NF-kB因子的抑制剂，具有抗炎，抗增殖免疫抑制，细胞保护和抗病毒活性，所选择的取代基选自 不影响NF-kB抑制活性。
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公开(公告)号：US06392100B1
公开(公告)日：2002-05-21
申请号：US09319743
申请日：1999-06-10
IPC分类号： C07C49537
CPC分类号： A61K31/122 , A61K31/42 , A61K2300/00
摘要： 2-Cyclopenten-1-one and its derivatives comprising the cyclopentenone nucleus as inhibitors of the NF-kB factor, with anti-inflammatory, anti-proliferative, immunosuppressive, cytoprotective and antiviral activity, the substituents being selected among the ones which do not affect the NF-kB inhibitory activity. Further the cyclopentenone derivative is a cyclopentenone compound which does not have two adjacent aliphatic side chains or a prostaglandin.
摘要翻译： 2-环戊烯-1-酮及其衍生物，其包含环戊烯酮核作为NF-kB因子的抑制剂，具有抗炎，抗增殖，免疫抑制，细胞保护和抗病毒活性，所述取代基选自不影响的 NF-kB抑制活性。 此外，环戊烯酮衍生物是不具有两个相邻的脂肪族侧链或前列腺素的环戊烯酮化合物。
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