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 。

公开(公告)号：US20100093743A1

公开(公告)日：2010-04-15

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： A61K31/498 ,  C07D215/12 ,  C07D263/56 ,  C07D241/36 ,  A61K31/47 ,  A61K31/423 ,  A61P35/00

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是酸性引导基团，独立地是主链长度为4以下的未取代或取代的饱和或不饱和的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 。

公开(公告)号：US07652036B2

公开(公告)日：2010-01-26

申请号：US10546153

申请日：2004-02-25

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 ,  A61K31/48

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 C17alkylene 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C17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 。

公开(公告)号：US20060079528A1

公开(公告)日：2006-04-13

申请号：US10546153

申请日：2004-02-25

申请人： Paul Finn ,  Ivars Kalvinsh ,  Einars Loza ,  Victor Andrianov ,  Olga Habarova ,  Daina Lolya ,  Irina Piskunova

发明人： Paul Finn ,  Ivars Kalvinsh ,  Einars Loza ,  Victor Andrianov ,  Olga Habarova ,  Daina Lolya ,  Irina Piskunova

IPC分类号： A61K31/517 ,  A61K31/502 ,  A61K31/498 ,  A61K31/4745 ,  A61K31/47 ,  C07D471/02

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 C17alkylene 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 a-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是酸引导基团，独立地是主链长度为4以下的未取代或取代的，饱和或不饱和的C 17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a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 。