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.

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.

公开(公告)号：US20050085515A1

公开(公告)日：2005-04-21

申请号：US10953106

申请日：2004-09-30

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. John 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. John 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 ,  C07D213/72 ,  A61K31/19 ,  A61K31/40 ,  A61K31/44

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 - ; 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。}

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。

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。

公开(公告)号：US07981895B2

公开(公告)日：2011-07-19

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： A61K31/497 ,  A61K31/4965

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。

公开(公告)号：US20100249197A1

公开(公告)日：2010-09-30

申请号：US12477493

申请日：2009-06-03

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 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 Bokaldere ,  Vija Gailite ,  Maxim Vorona ,  Victor Andrianov ,  Daina Lolya ,  Valentina Semenikhina ,  Andris Amolins ,  C. John Harris ,  James E.S. Duffy

IPC分类号： A61K31/4406 ,  C07C259/06 ,  A61K31/165 ,  A61P35/00 ,  A61P17/06 ,  C07C259/08 ,  C07D317/54 ,  A61K31/36 ,  C07D213/56 ,  C07D307/54 ,  A61K31/341

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 psorias

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，并且例如抑制增殖性疾病如癌症和牛皮癣

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。

公开(公告)号：US20110275810A1

公开(公告)日：2011-11-10

申请号：US13184869

申请日：2011-07-18

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： C07D295/26 ,  C07D405/10 ,  C07D403/04 ,  C07D401/04

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。

公开(公告)号：US07880020B2

公开(公告)日：2011-02-01

申请号：US12477493

申请日：2009-06-03

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： C07D333/36 ,  C07D333/22 ,  C07D307/02

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 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 psorias.

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，并且例如抑制增殖性疾病如癌症和牛皮癣。