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1. 发明授权

US07569724B2 Carbamic acid compounds comprising an amide linkage as HDAC inhibitors 失效
标题翻译：包含酰胺键作为HDAC抑制剂的氨基甲酸化合物
公开(公告)号：US07569724B2
公开(公告)日：2009-08-04
申请号：US10381791
申请日：2001-09-27
申请人： Clare J Watkins , Maria Rosario Romero-Martin , Kathryn G Moore , James Ritchie , Paul W Finn , Ivars Kalvinsh , Einars Loza , Igor Starchenkov , Klara Dikovska , Rasma M Bokaldere , Vija Gailite , Maxim Vorona , Victor Andrianov , Daina Lolya , Valentina Semenikhina , Andris Amolins , C. John Harris , James E. S. Duffy
发明人： Clare J Watkins , Maria Rosario Romero-Martin , Kathryn G Moore , James Ritchie , Paul W Finn , Ivars Kalvinsh , Einars Loza , Igor Starchenkov , Klara Dikovska , Rasma M Bokaldere , Vija Gailite , Maxim Vorona , Victor Andrianov , Daina Lolya , Valentina Semenikhina , Andris Amolins , C. John Harris , James E. S. Duffy
IPC分类号： C07C239/00
CPC分类号： C07D207/337 , A61K31/16 , A61K31/195 , A61K31/198 , A61K31/277 , A61K31/38 , A61K31/381 , A61K31/426 , C07C233/49 , C07C233/83 , C07C235/34 , C07C237/36 , C07C255/57 , C07C259/06 , C07C259/08 , C07C2603/18 , C07D207/40 , C07D207/404 , C07D209/14 , C07D209/16 , C07D209/18 , C07D209/22 , C07D213/06 , C07D213/55 , C07D213/56 , C07D233/04 , C07D233/08 , C07D235/14 , C07D235/24 , C07D271/06 , C07D307/34 , C07D307/54 , C07D317/60 , C07D333/24 , C07D333/60 , C07D403/12 , Y02A50/411
摘要： This invention pertains to certain active carbamic acid compounds which inhibit HDAC activity and which have the formula (1) wherein: A is an aryl group; Q1 is an aryl leader group having a backbone of at least 2 carbon atoms; J is an amide linkage selected from: —NR1C(═O)— and —C(═O)NR1-; R1 is an amido substituent; and, Q2 is an acid leader group; and pharmaceutically acceptable salts, solvates, amides, esters, ethers, chemically protected forms, and prodrugs thereof. The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo, to inhibit HDAC, and, e.g., to inhibit proliferative conditions, such as cancer and psoriasis.
摘要翻译：本发明涉及抑制HDAC活性的一些活性氨基甲酸化合物，其具有式（1）其中：A为芳基; Q1是具有至少2个碳原子的骨架的芳基前导基团; J是选自：-NR 1 C（-O） - 和-C（-O）NR 1 - 的酰胺键; R1是酰氨基取代基; 而Q2是酸性引导组; 和其药学上可接受的盐，溶剂合物，酰胺，酯，醚，化学保护形式及其前药。本发明还涉及包含这种化合物的药物组合物，以及这些化合物和组合物在体外和体内的用途，以抑制HDAC，并且例如抑制增殖性疾病如癌症和牛皮癣。

2. 发明授权

US07557140B2 Carbamic acid compounds comprising a sulfonamide linkage as HDAC inhibitors 有权
标题翻译：包含磺酰胺键作为HDAC抑制剂的氨基甲酸化合物
公开(公告)号：US07557140B2
公开(公告)日：2009-07-07
申请号：US12030397
申请日：2008-02-13
申请人： Ivars Kalvinsh , Einars Loza , Vija Gailite
发明人： Ivars Kalvinsh , Einars Loza , Vija Gailite
IPC分类号： A61K31/215 , A61K31/18
CPC分类号： C07D213/40 , C07C311/06 , C07C311/13 , C07C311/16 , C07C311/19 , C07C311/20 , C07C311/21 , C07C311/29 , C07C2602/08 , C07D209/88 , C07D213/42 , C07D213/65 , C07D213/71 , C07D307/52 , C07D317/58
摘要： This invention pertains to certain active carbamic acid compounds which inhibit HDAC activity and which have the following formula: (I) A is an aryl group; Q1 is a covalent bond or an aryl leader group; J is a sulfonamide linkage selected from: —S(═O)2NR1— and —NR1S(═O)2—; R1 is a sulfonamido substituent; and, Q2 is an acid leader group; with the proviso that if J is —S(═O)2NR1—, then Q1 is an aryl leader group; and pharmaceutically acceptable salts, solvates, amides, esters, ethers, chemically protected forms, and prodrugs thereof. The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo, to inhibit HDAC, and, e.g., to inhibit proliferative conditions, such as cancer and psoriasis.
摘要翻译：本发明涉及抑制HDAC活性的一些活性氨基甲酸化合物，其具有下式：（I）A为芳基; Q1是共价键或芳基引发基团; J是选自以下的磺酰胺键：-S（-O）2 NR 1 - 和-NR 1 S（-O）2 - ; R1是亚磺酰氨基取代基; 而Q2是酸性引导组; 条件是如果J是-S（-O）2 NR 1，则Q1是芳基前导基团; 和其药学上可接受的盐，溶剂合物，酰胺，酯，醚，化学保护形式及其前药。本发明还涉及包含这种化合物的药物组合物，以及这些化合物和组合物在体外和体内的用途，以抑制HDAC，并且例如抑制增殖性疾病如癌症和牛皮癣。

3. 发明申请

US20050107445A1 Carbamic acid compounds comprising a sulfonamide linkage as HDAC inhibitors 审中-公开
公开(公告)号：US20050107445A1
公开(公告)日：2005-05-19
申请号：US10811332
申请日：2004-03-29
申请人： Clare Watkins , Maria Rosario Romero-Martin , Kathryn Moore , James Ritchie , Paul Finn , Ivars Kalvinsh , Einars Loza , Klara Dikovska , Vija Gailite , Maxim Vorona , Irina Piskunova , Igor Starchenkov , Victor Andrianov , C. Harris , James Duffy
发明人： Clare Watkins , Maria Rosario Romero-Martin , Kathryn Moore , James Ritchie , Paul Finn , Ivars Kalvinsh , Einars Loza , Klara Dikovska , Vija Gailite , Maxim Vorona , Irina Piskunova , Igor Starchenkov , Victor Andrianov , C. Harris , James Duffy
IPC分类号： A61K31/341 , A61K31/403 , A61K31/4406 , A61P17/06 , A61P35/00 , A61P43/00 , C07C311/06 , C07C311/08 , C07C311/10 , C07C311/13 , C07C311/16 , C07C311/17 , C07C311/19 , C07C311/20 , C07C311/21 , C07C311/29 , C07D209/82 , C07D209/88 , C07D213/40 , C07D213/42 , C07D213/65 , C07D213/71 , C07D307/52 , C07D317/58 , A61K31/44 , A61K31/19 , A61K31/4015 , C07C311/35
CPC分类号： C07D213/40 , C07C311/06 , C07C311/13 , C07C311/16 , C07C311/19 , C07C311/20 , C07C311/21 , C07C311/29 , C07C2602/08 , C07D209/88 , C07D213/42 , C07D213/65 , C07D213/71 , C07D307/52 , C07D317/58
摘要： This invention pertains to certain active carbamic acid compounds which inhibit HDAC activity and which have the following formula: (I) A is an aryl group; Q1 is a covalent bond or an aryl leader group; J is a sulfonamide linkage selected from: —S(═O)2NR1— and —NR1S(═O)2—; R1 is a sulfonamido substituent; and, Q2 is an acid leader group; with the proviso that if J is —S(═O)2NR1—, then Q1 is an aryl leader group; and pharmaceutically acceptable salts, solvates, amides, esters, ethers, chemically protected forms, and prodrugs thereof. The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo, to inhibit HDAC, and, e.g., to inhibit proliferative conditions, such as cancer and psoriasis.

4. 发明授权

US06888027B2 Carbamic acid compounds comprising a sulfonamide linkage as HDAC inhibitors 有权
标题翻译：包含磺酰胺键作为HDAC抑制剂的氨基甲酸化合物
公开(公告)号：US06888027B2
公开(公告)日：2005-05-03
申请号：US10381790
申请日：2001-09-27
申请人： Clare J Watkins , Maria Rosario Romero-Martin , Kathryn G Moore , James Ritchie , Paul W Finn , Ivars Kalvinsh , Einars Loza , Klara Dikovska , Vija Gailite , Maxim Vorona , Irina Piskunova , Igor Starchenkov , Victor Andrianov , C. John Harris , James E. S. Duffy
发明人： Clare J Watkins , Maria Rosario Romero-Martin , Kathryn G Moore , James Ritchie , Paul W Finn , Ivars Kalvinsh , Einars Loza , Klara Dikovska , Vija Gailite , Maxim Vorona , Irina Piskunova , Igor Starchenkov , Victor Andrianov , C. John Harris , James E. S. Duffy
IPC分类号： A61K31/341 , A61K31/403 , A61K31/4406 , A61P17/06 , A61P35/00 , A61P43/00 , C07C311/06 , C07C311/08 , C07C311/10 , C07C311/13 , C07C311/16 , C07C311/17 , C07C311/19 , C07C311/20 , C07C311/21 , C07C311/29 , C07D209/82 , C07D209/88 , C07D213/40 , C07D213/42 , C07D213/65 , C07D213/71 , C07D307/52 , C07D317/58 , A01N37/28
CPC分类号： C07D213/40 , C07C311/06 , C07C311/13 , C07C311/16 , C07C311/19 , C07C311/20 , C07C311/21 , C07C311/29 , C07C2602/08 , C07D209/88 , C07D213/42 , C07D213/65 , C07D213/71 , C07D307/52 , C07D317/58
摘要： This invention pertains to certain active carbamic acid compounds which inhibit HDAC activity and which have the following formula: (I) A is an aryl group; Q1 is a covalent bond or an aryl leader group; J is a sulfonamide linkage selected from: —S(═O)2NR1— and —NR1S(═O)2—; R1 is a sulfonamido substituent; and, Q2 is an acid leader group; with the proviso that if J is —S(═O)2NR1—, then Q1 is an aryl leader group; and pharmaceutically acceptable salts, solvates, amides, esters, ethers, chemically protected forms, and prodrugs thereof. The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo, to inhibit HDAC, and, e.g., to inhibit proliferative conditions, such as cancer and psoriasis.
摘要翻译：本发明涉及抑制HDAC活性的一些活性氨基甲酸化合物，其具有下式：（I）A为芳基; Q 1是共价键或芳基前导基团; J是选自以下的磺酰胺键：-S（-O）2 NR 1 - 和-NR 1 S（-O） > 2 - ; R1是亚磺酰氨基取代基; 而Q 2是酸性引导基团; 条件是如果J是-S（-O）2 NR 1 - ，则Q 1是芳基前导基团; 和其药学上可接受的盐，溶剂合物，酰胺，酯，醚，化学保护形式及其前药。本发明还涉及包含这种化合物的药物组合物，以及这些化合物和组合物在体外和体内的用途，以抑制HDAC，并且例如抑制增殖性疾病如癌症和牛皮癣。

5. 发明申请

US20100029646A1 PRODRUGS OF DIPHENYL OX-INDOL-2-ONE COMPOUNDS 审中-公开
标题翻译：二苯氧基-2-二醇化合物的制备方法
公开(公告)号：US20100029646A1
公开(公告)日：2010-02-04
申请号：US12518545
申请日：2007-12-11
申请人： Mette Knak Christensen , Fredrik Bjoerkling , Martins Ikaunieks , Andrei Zaichenko , Vija Gailite , Einars Loza , Ivars Kalvinsh , Marina Madre
发明人： Mette Knak Christensen , Fredrik Bjoerkling , Martins Ikaunieks , Andrei Zaichenko , Vija Gailite , Einars Loza , Ivars Kalvinsh , Marina Madre
IPC分类号： A61K31/404 , C07D209/34 , C07D403/06 , C07D413/06 , A61P35/00 , A61K31/496 , A61K31/5377
CPC分类号： C07D209/34
摘要： The present application discloses prodrugs of substituted 3,3-diphenyl-1,3-dihydro-indol-2-one compounds having the general formula (I). The 4-position of the phenyl moieties and the N-position of the indole represent useful handles for the introduction of particular prodrug groups, in particular those comprising an amino acid moiety. The prodrug compounds are believed to be useful for the treatment of cancer in a mammal, possibly in combination with one or more other chemotherapeutic agents. The application also discloses the compounds for use in a method of treating a mammal suffering from or being susceptible to cancer
摘要翻译：本申请公开了具有通式（I）的取代的3,3-二苯基-1,3-二氢 - 吲哚-2-酮化合物的前药。苯基部分的4-位和吲哚的N-位表示用于引入特定前药基团，特别是包含氨基酸部分的那些的有用的手段。认为前药化合物可用于治疗哺乳动物中的癌症，可能与一种或多种其它化学治疗剂组合。本申请还公开了用于治疗患有或易患癌症的哺乳动物的方法中的化合物

6. 发明申请

US20080269237A1 CARBAMIC ACID COMPOUNDS COMPRISING A PIPERAZINE LINKAGE AS HDAC INHIBITORS 有权
标题翻译：包含作为HDAC抑制剂的哌嗪连接物的碳酸化合物
公开(公告)号：US20080269237A1
公开(公告)日：2008-10-30
申请号：US12165686
申请日：2008-07-01
申请人： Clare J. WATKINS , Maria-Rosario Romero-Martin , James Ritchie , Paul W. Finn , Ivars Kalvinsh , Einars Loza , Klara Dikovska , Igor Starchenkov , Daina Lolya , Vija Gailite
发明人： Clare J. WATKINS , Maria-Rosario Romero-Martin , James Ritchie , Paul W. Finn , Ivars Kalvinsh , Einars Loza , Klara Dikovska , Igor Starchenkov , Daina Lolya , Vija Gailite
IPC分类号： A61K31/506 , A61K31/495 , A61P35/00 , C12N9/99 , A61P25/28 , A61P25/16
CPC分类号： C07D213/74 , C07D239/42 , C07D295/185 , C07D295/192 , C07D295/26 , C07D317/58 , C07D333/60
摘要： This invention pertains to certain carbamic acid compounds which inhibit HDAC (histone deacetylase) activity of the following formula: The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo, to inhibit HDAC, and in the treatment of conditions mediated by HDAC, cancer, proliferative conditions, psoriasis, etc.
摘要翻译：本发明涉及抑制下式的HDAC（组蛋白脱乙酰酶）活性的某些氨基甲酸化合物：本发明还涉及包含这些化合物的药物组合物，以及这些化合物和组合物在体外和体内的用途抑制HDAC，以及治疗由HDAC，癌症，增殖性病症，牛皮癣等介导的病症。

7. 发明授权

US07407988B2 Carbamic acid compounds comprising a sulfonamide linkage as HDAC inhibitors 有权
标题翻译：包含磺酰胺键作为HDAC抑制剂的氨基甲酸化合物
公开(公告)号：US07407988B2
公开(公告)日：2008-08-05
申请号：US11516620
申请日：2006-09-07
申请人： Ivars Kalvinsh , Einars Loza , Vija Gailite
发明人： Ivars Kalvinsh , Einars Loza , Vija Gailite
IPC分类号： A61K31/19 , C07C259/04
CPC分类号： C07D213/40 , C07C311/06 , C07C311/13 , C07C311/16 , C07C311/19 , C07C311/20 , C07C311/21 , C07C311/29 , C07C2602/08 , C07D209/88 , C07D213/42 , C07D213/65 , C07D213/71 , C07D307/52 , C07D317/58
摘要： This invention pertains to certain active carbamic acid compounds which inhibit HDAC activity and which have the following formula: (1) A is an aryl group; Q1 is a covalent bond or an aryl leader group; J is a sulfonamide linkage selected from: —S(═O)2NR1— and —NR1S(═O)2—; R1 is a sulfonamido substituent; and, Q2 is an acid leader group; with the proviso that if J is —S(═O)2NR1—, then Q1 is an aryl leader group; and pharmaceutically acceptable salts, solvates, amides, esters, ethers, chemically protected forms, and prodrugs thereof. The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo, to inhibit HDAC, and, e.g., to inhibit proliferative conditions, such as cancer and psoriasis.
摘要翻译：本发明涉及某些抑制HDAC活性的活性氨基甲酸化合物，具有下式：（1）A为芳基; Q 1是共价键或芳基前导基团; J是选自以下的磺酰胺键：-S（-O）2 NR 1 - 和-NR 1 S（-O）_{2 - ; R 1是磺酰胺基取代基; 而Q 2是酸性引导基团; 条件是如果J是-S（-O）2 NR 1 - ，则Q 1是芳基前导基团; 和其药学上可接受的盐，溶剂合物，酰胺，酯，醚，化学保护形式及其前药。本发明还涉及包含这种化合物的药物组合物，以及这些化合物和组合物在体外和体内的用途，以抑制HDAC，并且例如抑制增殖性疾病如癌症和牛皮癣。}

8. 发明申请

US20050143385A1 Carbamic acid compounds comprising a piperazine linkage as hdac inhibitors 失效
公开(公告)号：US20050143385A1
公开(公告)日：2005-06-30
申请号：US10509732
申请日：2003-04-03
申请人： Clare Watkins , Maria-Rosario Romero-Martin , James Ritchie , Paul Finn , Ivars Kalvinsh , Einars Loza , Klar Dikovska , Igor Starchenkov , Daina Lolya , Vija Gailite
发明人： Clare Watkins , Maria-Rosario Romero-Martin , James Ritchie , Paul Finn , Ivars Kalvinsh , Einars Loza , Klar Dikovska , Igor Starchenkov , Daina Lolya , Vija Gailite
IPC分类号： C07D295/16 , A61K31/495 , A61K31/496 , A61K31/506 , A61P17/06 , A61P35/00 , A61P43/00 , C07D209/14 , C07D209/16 , C07D209/18 , C07D209/42 , C07D213/36 , C07D213/74 , C07D239/42 , C07D241/04 , C07D295/18 , C07D295/185 , C07D295/192 , C07D295/22 , C07D295/26 , C07D317/58 , C07D333/60 , C07D43/02
CPC分类号： C07D213/74 , C07D239/42 , C07D295/185 , C07D295/192 , C07D295/26 , C07D317/58 , C07D333/60
摘要： This invention pertains to certain carbamic acid compounds which inhibit HDAC (histone deacetylase) activity of the following formula: wherein: Cy is independently a cyclyl group; Q1 is independently a covalent bond or cyclyl leader group; the piperazin-1,4-diyl group is optionally substituted; J1 is independently a covalent bond or —C(═;O)—; J2 is independently —C(═O)— or —S(═O)2—; Q2 is independently an acid leader group; wherein: Cy is independently: C3-20carbocyclyl, C3-20heterocyclyl, or C5-20aryl; and is optionally substituted; Q1 is independently: a covalent bond; C1-7alkylene; or C1-7alkylene-X—C1-7alkylene, —X—C1-7alkylene, or C1-7alkylene-X—, wherein X is —O— or —S—; and is optionally substituted; Q2 is independently: C4-8alkylene; and is optionally substituted; and has a backbone length of at least 4 atoms; or: Q2 is independently: C5-20arylene; C5-20arylene-C1-7alkylene; C1-7alkylene-C5-20arylene; or, C1-7alkylene-C5-20arylene-C1-7alkylene; and is optionally substituted; and has a backbone length of at least 4 atoms; or a pharmaceutically acceptable salt, solvate, amide, ester, ether, chemically protected form, or prodrug thereof. The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo, to inhibit HDAC, and in the treatment of conditions mediated by HDAC, cancer, proliferative conditions, psoriasis, etc.

9. 发明授权

US08071620B2 Carbamic acid compounds comprising a bicyclic heteroaryl group as HDAC inhibitors 失效
标题翻译：包含双环杂芳基作为HDAC抑制剂的氨基甲酸化合物
公开(公告)号：US08071620B2
公开(公告)日：2011-12-06
申请号：US12636949
申请日：2009-12-14
申请人： Paul W. Finn , Ivars Kalvinsh , Einars Loza , Victor Andrianov , Olga Habarova , Daina Lolya , Irina Piskunova
发明人： Paul W. Finn , Ivars Kalvinsh , Einars Loza , Victor Andrianov , Olga Habarova , Daina Lolya , Irina Piskunova
IPC分类号： C07D215/38 , A61K31/04
CPC分类号： C07D263/56 , C07D215/12 , C07D215/14 , C07D215/18 , C07D215/20 , C07D241/42 , C07D241/44 , C07D277/64
摘要： This invention pertains to certain carbamic acid compounds of the following formula, which inhibit HDAC (histone deacetylase) activity wherein: A is independently an unsubstituted or substituted bicyclic C9-10heteroaryl group (e.g., quinolinyl; quinoxalinyl; benzoxazolyl; benzothiazolyl); Q is an acid leader group, and is independently an unsubstituted or substituted, saturated or unsaturated C1-7alkylene group having a backbone length of 4 or less; with the proviso that if A is unsubstituted benzothiazol-2-yl, then Q is an unsaturated group; and with the proviso that if A is unsubstituted quinolin-6-yl, then Q is unsubstituted at the α-position; and with the proviso that A is not benzimidazol-2-yl; and pharmaceutically acceptable salts, solvates, amides, esters, ethers, chemically protected forms, and prodrugs thereof. The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo, to inhibit HDAC, and in the treatment of conditions mediated by HDAC, cancer, proliferative conditions, psoriasis, etc.
摘要翻译：本发明涉及抑制HDAC（组蛋白脱乙酰酶）活性的某些下式的氨基甲酸化合物，其中：A独立地是未取代或取代的双环C 9-10杂芳基（例如喹啉基;喹喔啉基;苯并恶唑基;苯并噻唑基）; Q为酸性引导基团，独立地为骨架长度为4以下的未取代或取代的饱和或不饱和C 1-7亚烷基; 条件是如果A是未取代的苯并噻唑-2-基，则Q是不饱和基团; 并且条件是如果A是未取代的喹啉-6-基，那么Q在α-位是未取代的; 并且条件是A不是苯并咪唑-2-基; 和其药学上可接受的盐，溶剂合物，酰胺，酯，醚，化学保护形式及其前药。本发明还涉及包含这些化合物的药物组合物，以及这些化合物和组合物在体外和体内的用途，以抑制HDAC，以及治疗由HDAC，癌症，增殖性病症，牛皮癣等介导的病症。

10. 发明申请

US20110105572A1 CARBAMIC ACID COMPOUNDS COMPRISING AN AMIDE LINKAGE AS HDAC INHIBITORS 审中-公开
标题翻译：包含作为HDAC抑制剂的酰胺链接的碳酸化合物
公开(公告)号：US20110105572A1
公开(公告)日：2011-05-05
申请号：US12983971
申请日：2011-01-04
申请人： Clare J. Watkins , Maria Rosario Romero-Martin , Kathryn G. Moore , James Ritchie , Paul W. Finn , Ivars Kalvinsh , Einars Loza , Igor Starchenkov , Klara Dikovska , Rasma M. Bokaldere , Vija Gailite , Maxim Vorona , Victor Andrianov , Daina Lolya , Valentina Semenikhina , Andris Amolins , C. John Harris , James E.S. Duffy
发明人： Clare J. Watkins , Maria Rosario Romero-Martin , Kathryn G. Moore , James Ritchie , Paul W. Finn , Ivars Kalvinsh , Einars Loza , Igor Starchenkov , Klara Dikovska , Rasma M. Bokaldere , Vija Gailite , Maxim Vorona , Victor Andrianov , Daina Lolya , Valentina Semenikhina , Andris Amolins , C. John Harris , James E.S. Duffy
IPC分类号： A61K31/165 , C07C259/06 , C07C259/08 , A61K31/167 , C07D317/60 , A61K31/36 , C07D213/56 , A61K31/4409 , C07D307/54 , A61K31/341 , A61K31/166 , C07D271/08 , A61K31/4245 , C07D207/337 , A61K31/40 , A61K31/4406 , C07D209/20 , A61K31/405 , C07D333/24 , A61K31/381 , A61P35/00 , C12N5/02
CPC分类号： C07D207/337 , A61K31/16 , A61K31/195 , A61K31/198 , A61K31/277 , A61K31/38 , A61K31/381 , A61K31/426 , C07C233/49 , C07C233/83 , C07C235/34 , C07C237/36 , C07C255/57 , C07C259/06 , C07C259/08 , C07C2603/18 , C07D207/40 , C07D207/404 , C07D209/14 , C07D209/16 , C07D209/18 , C07D209/22 , C07D213/06 , C07D213/55 , C07D213/56 , C07D233/04 , C07D233/08 , C07D235/14 , C07D235/24 , C07D271/06 , C07D307/34 , C07D307/54 , C07D317/60 , C07D333/24 , C07D333/60 , C07D403/12 , Y02A50/411
摘要： This invention pertains to certain active carbamic acid compounds which inhibit HDAC activity and which have the following formula: wherein: A is a C5-20heteroaryl or C5-20carboaryl group and is optionally substituted; Q1 is a C2-7alkylene group having a backbone of at least 2 carbon atoms, and is optionally substituted; J is —N(R1)C(═O)— or —C(═O)N(R1)—; R1 is hydrogen, C1-7alkyl, C3-20heterocyclyl, or C5-20aryl; and, Q2 is C1-7alkylene, C5-20arylene, C5-20arylene-C1-7alkylene, or C1-7alkylene-C5-20arylene having a backbone of at least 3 carbon atoms, and is optionally substituted; and pharmaceutically acceptable salts thereof. The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo, to inhibit HDAC, and, e.g., to treat proliferative conditions, such as cancer and psoriasis.
摘要翻译：本发明涉及一些抑制HDAC活性的活性氨基甲酸化合物，其具有下式：其中：A为C 5-20杂芳基或C 5-20碳氢芳基并且任选被取代; Q1是具有至少2个碳原子的主链的C2-7亚烷基，并且任选被取代; J是-N（R 1）C（= O） - 或-C（= O）N（R 1） - ; R 1是氢，C 1-7烷基，C 3-20杂环基或C 5-20芳基; 并且Q2是具有至少3个碳原子的主链的C 1-7亚烷基，C 5-20亚芳基，C 5-20亚芳基-C 1-7亚烷基或C 1-7亚烷基-C 5-20亚芳基，并且任选被取代; 及其药学上可接受的盐。本发明还涉及包含这些化合物的药物组合物，以及这些化合物和组合物在体外和体内的用途，以抑制HDAC，并且例如治疗增殖性疾病如癌症和牛皮癣。

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