公开(公告)号：US07750042B2

公开(公告)日：2010-07-06

申请号：US12077729

申请日：2008-03-20

申请人： Keizo Koya ,  Lijun Sun ,  Shoujun Chen ,  Noriaki Tatsuta ,  Yaming Wu ,  Mitsunori Ono ,  Zhi-Qiang Xia

发明人： Keizo Koya ,  Lijun Sun ,  Shoujun Chen ,  Noriaki Tatsuta ,  Yaming Wu ,  Mitsunori Ono ,  Zhi-Qiang Xia

IPC分类号： A61K31/335 ,  A61K31/20 ,  C07C327/38 ,  C07C243/18

CPC分类号： C07D307/68 ,  A45D2008/006 ,  A61K31/337 ,  A61K31/505 ,  A61K31/53 ,  A61K31/5377 ,  A61K47/58 ,  C07C327/56 ,  C07C2601/02 ,  C07C2601/04 ,  C07C2601/08 ,  C07C2601/14 ,  C07D209/42 ,  C07D209/44 ,  C07D213/83 ,  C07D261/18 ,  C07D333/38 ,  C07D333/68

摘要： One embodiment of the present invention is a compound represented by the Structural Formula (I): Y is a covalent bond of a substituted or unsubstituted straight chained hydrocarbyl group. In addition, Y, taken together with both >C═Z groups to which it is bonded, is a substituted or unsubstituted aromatic group. Preferably, Y is a covalent bond or —C(R7R8)—. R1 is an aliphatic group, a substituted aliphatic group, a non-aromatic heterocyclic group, or a substituted non-aromatic heterocyclic group, R2-R4 are independently —H, an aliphatic group, a substituted aliphatic group, a non-aromatic heterocyclic group, a substituted non-aromatic heterocyclic group, an aryl group or a substituted aryl group, or R1 and R3 taken together with the carbon and nitrogen atoms to which they are bonded, and/or R2 and R4 taken together with the carbon and nitrogen atoms to which they are bonded, form a non-aromatic heterocyclic ring optionally fused to an aromatic ring. R5-R6 are independently —H, an aliphatic group, a substituted aliphatic group, an aryl group or a substituted aryl group. R7 and R8 are each independently —H, an aliphatic or substituted aliphatic group, or R7 is —H and R8 is a substituted or unsubstituted aryl group, or, R7 and R8, taken together, are a C2-C6 substituted or unsubstituted alkylene group. Z is ═O or ═S. Also disclosed are pharmaceutical compositions comprising the compound of the present invention and a pharmaceutically acceptable carrier or diluent.

摘要翻译： 本发明的一个实施方案是由结构式（I）表示的化合物：Y是取代或未取代的直链烃基的共价键。 此外，Y与它所键合的两个> C = Z基团一起是取代或未取代的芳族基团。 优选Y为共价键或-C（R 7 R 8） - 。 R1是脂肪族基团，取代脂肪族基团，非芳族杂环基团或取代的非芳族杂环基团，R2-R4独立地是-H，脂肪族基团，取代的脂肪族基团，非芳香族杂环基 ，取代的非芳族杂环基，芳基或取代的芳基，或者R 1和R 3与它们所键合的碳原子和氮原子一起，和/或R 2和R 4与碳和氮原子一起 形成与芳环稠合的非芳族杂环。 R5-R6独立地是-H，脂族基团，取代的脂族基团，芳基或取代的芳基。 R 7和R 8各自独立地为-H，脂族或取代的脂族基团，或者R 7为-H且R 8为取代或未取代的芳基，或者R 7和R 8一起为C 2 -C 6取代或未取代的亚烷基 。 Z为═O或═S。 还公开了包含本发明化合物和药学上可接受的载体或稀释剂的药物组合物。

公开(公告)号：US20060116374A1

公开(公告)日：2006-06-01

申请号：US11244427

申请日：2005-10-05

申请人： Keizo Koya ,  Lijun Sun ,  Shoujun Chen ,  Noriaki Tatsuta ,  Yaming Wu ,  Mitsunori Ono ,  Zhi-Qiang Xia

发明人： Keizo Koya ,  Lijun Sun ,  Shoujun Chen ,  Noriaki Tatsuta ,  Yaming Wu ,  Mitsunori Ono ,  Zhi-Qiang Xia

IPC分类号： A61K31/5377 ,  A61K31/53 ,  A61K31/505 ,  A61K31/337

CPC分类号： C07D307/68 ,  A45D2008/006 ,  A61K31/337 ,  A61K31/505 ,  A61K31/53 ,  A61K31/5377 ,  A61K47/58 ,  C07C327/56 ,  C07C2601/02 ,  C07C2601/04 ,  C07C2601/08 ,  C07C2601/14 ,  C07D209/42 ,  C07D209/44 ,  C07D213/83 ,  C07D261/18 ,  C07D333/38 ,  C07D333/68

摘要： One embodiment of the present invention is a compound represented by the Structural Formula (I): Y is a covalent bond of a substituted or unsubstituted straight chained hydrocarbyl group. In addition, Y, taken together with both >C=Z groups to which it is bonded, is a substituted or unsubstituted aromatic group. Preferably, Y is a covalent bond or —C(R7R8)—. R1 is an aliphatic group, a substituted aliphatic group, a non-aromatic heterocyclic group, or a substituted non-aromatic heterocyclic group, R2-R4 are independently —H, an aliphatic group, a substituted aliphatic group, a non-aromatic heterocyclic group, a substituted non-aromatic heterocyclic group, an aryl group or a substituted aryl group, or R1 and R3 taken together with the carbon and nitrogen atoms to which they are bonded, and/or R2 and R4 taken together with the carbon and nitrogen atoms to which they are bonded, form a non-aromatic heterocyclic ring optionally fused to an aromatic ring. R5-R6 are independently —H, an aliphatic group, a substituted aliphatic group, an aryl group or a substituted aryl group. R7 and R8 are each independently —H, an aliphatic or substituted aliphatic group, or R7 is —H and R8 is a substituted or unsubstituted aryl group, or, R7 and R8, taken together, are a C2-C6 substituted or unsubstituted alkylene group. Z is ═O or ═S. Also disclosed are pharmaceutical compositions comprising the compound of the present invention and a pharmaceutically acceptable carrier or diluent.

摘要翻译： 本发明的一个实施方案是由结构式（I）表示的化合物：Y是取代或未取代的直链烃基的共价键。 此外，Y与它所键合的两个> C = Z基团一起是取代或未取代的芳族基团。 优选地，Y是共价键或-C（R 7 R 8） - 。 R 1是脂族基团，取代的脂族基团，非芳族杂环基团或取代的非芳香族杂环基团，R 2 -R 4 独立地，-H，脂族基团，取代的脂族基团，非芳香族杂环基，取代的非芳族杂环基，芳基或取代的芳基，或R 1， SUB和R 3与它们所键合的碳原子和氮原子一起，和/或R 2和R 4结合在一起 与其键合的碳原子和氮原子形成任选地稠合到芳香环的非芳族杂环。 R 5 -R 6独立地是-H，脂族基团，取代的脂族基团，芳基或取代的芳基。 R 7和R 8各自独立地为-H，脂族或取代的脂族基团或R 7为-H， 8是取代或未取代的芳基，或者R 7和R 8一起是C2-C6取代或未取代的亚烷基。 Z是-O或-S。 还公开了包含本发明化合物和药学上可接受的载体或稀释剂的药物组合物。

公开(公告)号：US07435843B2

公开(公告)日：2008-10-14

申请号：US11440429

申请日：2006-05-24

申请人： Shoujun Chen ,  Lijun Sun ,  Zhi-Qiang Xia ,  Keizo Koya ,  Mitsunori Ono

发明人： Shoujun Chen ,  Lijun Sun ,  Zhi-Qiang Xia ,  Keizo Koya ,  Mitsunori Ono

IPC分类号： C07C327/56

CPC分类号： C07D213/77 ,  C07C327/56 ,  C07C2601/14 ,  C07D209/42 ,  C07D209/44 ,  C07D213/83 ,  C07D261/18 ,  C07D307/54 ,  C07D333/38 ,  Y02P20/55

摘要： Disclosed is a method of preparing a thiohydrazide product compound from a hydrazide starting compound. The hydrazide starting compound is represented by Structural Formula (I): The thiohydrazide product compound is represented by Structural Formula (II): In Structural Formulas (I)-(II), R1 and R2 are independently an aliphatic group, a substituted aliphatic group, an aryl group or a substituted aryl group, or R1 and R2 taken together with the carbon and nitrogen atoms to which they are bonded, form a non-aromatic heterocyclic ring optionally fused to an aromatic ring. When R2 is an aryl group or a substituted aryl group, then R5 is a hydrazine protecting group; and when R2 is an aliphatic or substituted aliphatic group, then R5 is —H or a hydrazine protecting group. R10 is —H or a substituted or unsubstituted alkyl group. The method comprising the step of reacting the starting compound with a thionylating reagent.

摘要翻译： 公开了从酰肼起始化合物制备硫代酰肼产物化合物的方法。 酰肼起始化合物由结构式（I）表示：硫代酰肼产物化合物由结构式（II）表示：在结构式（I） - （II）中，R 1和R 2 > 2 独立地是脂族基团，取代的脂族基团，芳基或取代的芳基，或R 1和R 2与 与它们键合的碳原子和氮原子形成任选地与芳环稠合的非芳族杂环。 当R 2是芳基或取代的芳基时，R 5是肼保护基; 当R 2是脂族或取代的脂族基团时，R 5是-H或肼保护基。 R 10是-H或取代或未取代的烷基。 该方法包括使起始化合物与亚硫酰化试剂反应的步骤。

公开(公告)号：US20060281811A1

公开(公告)日：2006-12-14

申请号：US11440429

申请日：2006-05-24

申请人： Shoujun Chen ,  Lijun Sun ,  Zhi-Qiang Xia ,  Keizo Koya ,  Mitsunori Ono

发明人： Shoujun Chen ,  Lijun Sun ,  Zhi-Qiang Xia ,  Keizo Koya ,  Mitsunori Ono

IPC分类号： A61K31/235 ,  A61K31/195

CPC分类号： C07D213/77 ,  C07C327/56 ,  C07C2601/14 ,  C07D209/42 ,  C07D209/44 ,  C07D213/83 ,  C07D261/18 ,  C07D307/54 ,  C07D333/38 ,  Y02P20/55

摘要： Disclosed is a method of preparing a thiohydrazide product compound from a hydrazide starting compound. The hydrazide starting compound is represented by Structural Formula (I): The thiohydrazide product compound is represented by Structural Formula (II): In Structural Formulas (I)-(II), R1 and R2 are independently an aliphatic group, a substituted aliphatic group, an aryl group or a substituted aryl group, or R1 and R2 taken together with the carbon and nitrogen atoms to which they are bonded, form a non-aromatic heterocyclic ring optionally fused to an aromatic ring. When R2 is an aryl group or a substituted aryl group, then R5 is a hydrazine protecting group; and when R2 is an aliphatic or substituted aliphatic group, then R5 is —H or a hydrazine protecting group. R10 is —H or a substituted or unsubstituted alkyl group. The method comprising the step of reacting the starting compound with a thionylating reagent.

摘要翻译： 公开了从酰肼起始化合物制备硫代酰肼产物化合物的方法。 酰肼起始化合物由结构式（I）表示：硫代酰肼产物化合物由结构式（II）表示：在结构式（I） - （II）中，R 1和R 2 > 2 独立地是脂族基团，取代的脂族基团，芳基或取代的芳基，或R 1和R 2与 与它们键合的碳原子和氮原子形成任选地与芳环稠合的非芳族杂环。 当R 2是芳基或取代的芳基时，R 5是肼保护基; 当R 2是脂族或取代的脂族基团时，R 5是-H或肼保护基。 R 10是-H或取代或未取代的烷基。 该方法包括使起始化合物与亚硫酰化试剂反应的步骤。

公开(公告)号：US07074952B2

公开(公告)日：2006-07-11

申请号：US10807919

申请日：2004-03-24

申请人： Shoujun Chen ,  Lijun Sun ,  Zhi-Qiang Xia ,  Keizo Koya ,  Mitsunori Ono

发明人： Shoujun Chen ,  Lijun Sun ,  Zhi-Qiang Xia ,  Keizo Koya ,  Mitsunori Ono

IPC分类号： C07C69/66 ,  C07C327/00 ,  A61K31/215 ,  A61K31/16

CPC分类号： C07D213/77 ,  C07C327/56 ,  C07C2601/14 ,  C07D209/42 ,  C07D209/44 ,  C07D213/83 ,  C07D261/18 ,  C07D307/54 ,  C07D333/38 ,  Y02P20/55

摘要： Disclosed is a method of preparing a thiohydrazide product compound from a hydrazide starting compound. The hydrazide starting compound is represented by Structural Formula (I): The thiohydrazide product compound is represented by Structural Formula (II): In Structural Formulas (I)–(II), R1 and R2 are independently an aliphatic group, a substituted aliphatic group, an aryl group or a substituted aryl group, or R1 and R2 taken together with the carbon and nitrogen atoms to which they are bonded, form a non-aromatic heterocyclic ring optionally fused to an aromatic ring. When R2 is an aryl group or a substituted aryl group, then R5 is a hydrazine protecting group; and when R2 is an aliphatic or substituted aliphatic group, then R5 is —H or a hydrazine protecting group. R10 is —H or a substituted or unsubstituted alkyl group. The method comprising the step of reacting the starting compound with a thionylating reagent.

公开(公告)号：US20080242702A1

公开(公告)日：2008-10-02

申请号：US12077729

申请日：2008-03-20

申请人： Keizo Koya ,  Lijun Sun ,  Shoujun Chen ,  Noriaki Tatsuta ,  Yaming Wu ,  Mitsunori Ono ,  Zhi-Qiang Xia

发明人： Keizo Koya ,  Lijun Sun ,  Shoujun Chen ,  Noriaki Tatsuta ,  Yaming Wu ,  Mitsunori Ono ,  Zhi-Qiang Xia

IPC分类号： A61K31/265 ,  C07C327/18 ,  C07D209/04 ,  A61K31/444 ,  A61P35/00 ,  A61K31/404 ,  C07D213/02

CPC分类号： C07D307/68 ,  A45D2008/006 ,  A61K31/337 ,  A61K31/505 ,  A61K31/53 ,  A61K31/5377 ,  A61K47/58 ,  C07C327/56 ,  C07C2601/02 ,  C07C2601/04 ,  C07C2601/08 ,  C07C2601/14 ,  C07D209/42 ,  C07D209/44 ,  C07D213/83 ,  C07D261/18 ,  C07D333/38 ,  C07D333/68

摘要： One embodiment of the present invention is a compound represented by the Structural Formula (I): Y is a covalent bond of a substituted or unsubstituted straight chained hydrocarbyl group. In addition, Y, taken together with both >C=Z groups to which it is bonded, is a substituted or unsubstituted aromatic group. Preferably, Y is a covalent bond or —C(R7R8)—. R1 is an aliphatic group, a substituted aliphatic group, a non-aromatic heterocyclic group, or a substituted non-aromatic heterocyclic group, R2-R4 are independently —H, an aliphatic group, a substituted aliphatic group, a non-aromatic heterocyclic group, a substituted non-aromatic heterocyclic group, an aryl group or a substituted aryl group, or R1 and R3 taken together with the carbon and nitrogen atoms to which they are bonded, and/or R2 and R4 taken together with the carbon and nitrogen atoms to which they are bonded, form a non-aromatic heterocyclic ring optionally fused to an aromatic ring. R5-R6 are independently —H, an aliphatic group, a substituted aliphatic group, an aryl group or a substituted aryl group. R7 and R8 are each independently —H, an aliphatic or substituted aliphatic group, or R7 is —H and R8 is a substituted or unsubstituted aryl group, or, R7 and R8, taken together, are a C2-C6 substituted or unsubstituted alkylene group. Z is ═O or ═S. Also disclosed are pharmaceutical compositions comprising the compound of the present invention and a pharmaceutically acceptable carrier or diluent.

摘要翻译： 本发明的一个实施方案是由结构式（I）表示的化合物：Y是取代或未取代的直链烃基的共价键。 此外，Y与它所键合的两个> C = Z基团一起是取代或未取代的芳族基团。 优选地，Y是共价键或-C（R 7 R 8） - 。 R 1是脂族基团，取代的脂族基团，非芳族杂环基团或取代的非芳香族杂环基团，R 2 -R 4 独立地，-H，脂族基团，取代的脂族基团，非芳香族杂环基，取代的非芳族杂环基，芳基或取代的芳基，或R 1， SUB和R 3与它们所键合的碳原子和氮原子一起，和/或R 2和R 4结合在一起 与其键合的碳原子和氮原子形成任选地稠合到芳香环的非芳族杂环。 R 5 -R 6独立地是-H，脂族基团，取代的脂族基团，芳基或取代的芳基。 R 7和R 8各自独立地为-H，脂族或取代的脂族基团或R 7为-H， 8是取代或未取代的芳基，或者R 7和R 8一起是C2-C6取代或未取代的亚烷基。 Z是-O或-S。 还公开了包含本发明化合物和药学上可接受的载体或稀释剂的药物组合物。

公开(公告)号：US07368473B2

公开(公告)日：2008-05-06

申请号：US11244427

申请日：2005-10-05

申请人： Keizo Koya ,  Lijun Sun ,  Shoujun Chen ,  Noriaki Tatsuta ,  Yaming Wu ,  Mitsunori Ono ,  Zhi-Qiang Xia

发明人： Keizo Koya ,  Lijun Sun ,  Shoujun Chen ,  Noriaki Tatsuta ,  Yaming Wu ,  Mitsunori Ono ,  Zhi-Qiang Xia

IPC分类号： A61K31/16 ,  A61K31/335

CPC分类号： C07D307/68 ,  A45D2008/006 ,  A61K31/337 ,  A61K31/505 ,  A61K31/53 ,  A61K31/5377 ,  A61K47/58 ,  C07C327/56 ,  C07C2601/02 ,  C07C2601/04 ,  C07C2601/08 ,  C07C2601/14 ,  C07D209/42 ,  C07D209/44 ,  C07D213/83 ,  C07D261/18 ,  C07D333/38 ,  C07D333/68

摘要： One embodiment of the present invention is a compound represented by the Structural Formula (I): Y is a covalent bond of a substituted or unsubstituted straight chained hydrocarbyl group. In addition, Y, taken together with both >C═Z groups to which it is bonded, is a substituted or unsubstituted aromatic group. Preferably, Y is a covalent bond or —C(R7R8)—.R1 is an aliphatic group, a substituted aliphatic group, a non-aromatic heterocyclic group, or a substituted non-aromatic heterocyclic group, R2-R4 are independently —H, an aliphatic group, a substituted aliphatic group, a non-aromatic heterocyclic group, a substituted non-aromatic heterocyclic group, an aryl group or a substituted aryl group, or R1 and R3 taken together with the carbon and nitrogen atoms to which they are bonded, and/or R2 and R4 taken together with the carbon and nitrogen atoms to which they are bonded, form a non-aromatic heterocyclic ring optionally fused to an aromatic ring.R5-R6 are independently —H, an aliphatic group, a substituted aliphatic group, an aryl group or a substituted aryl group.R7 and R8 are each independently —H, an aliphatic or substituted aliphatic group, or R7 is —H and R8 is a substituted or unsubstituted aryl group, or, R7 and R8, taken together, are a C2-C6 substituted or unsubstituted alkylene group.Z is ═O or ═S.Also disclosed are pharmaceutical compositions comprising the compound of the present invention and a pharmaceutically acceptable carrier or diluent.

摘要翻译： 本发明的一个实施方案是由结构式（I）表示的化合物：Y是取代或未取代的直链烃基的共价键。 此外，Y与它所键合的两个> C-Z基团一起是取代或未取代的芳族基团。 优选地，Y是共价键或-C（R 7 R 8） - 。 R 1是脂族基团，取代的脂族基团，非芳族杂环基团或取代的非芳香族杂环基团，R 2 -R 4 独立地，-H，脂族基团，取代的脂族基团，非芳香族杂环基，取代的非芳族杂环基，芳基或取代的芳基，或R 1， SUB和R 3与它们所键合的碳原子和氮原子一起，和/或R 2和R 4结合在一起 与其键合的碳原子和氮原子形成任选地稠合到芳香环的非芳族杂环。 R 5 -R 6独立地是-H，脂族基团，取代的脂族基团，芳基或取代的芳基。 R 7和R 8各自独立地为-H，脂族或取代的脂族基团或R 7为-H， 8是取代或未取代的芳基，或者R 7和R 8一起是C2-C6取代或未取代的亚烷基。 Z是-O或-S。 还公开了包含本发明化合物和药学上可接受的载体或稀释剂的药物组合物。

公开(公告)号：US06825235B2

公开(公告)日：2004-11-30

申请号：US10193076

申请日：2002-07-10

申请人： Shoujun Chen ,  Lijun Sun ,  Zhi-Qiang Xia ,  Keizo Koya ,  Mitsunori Ono

发明人： Shoujun Chen ,  Lijun Sun ,  Zhi-Qiang Xia ,  Keizo Koya ,  Mitsunori Ono

IPC分类号： A61K3116

CPC分类号： C07D213/77 ,  C07C327/56 ,  C07C2601/14 ,  C07D209/42 ,  C07D209/44 ,  C07D213/83 ,  C07D261/18 ,  C07D307/54 ,  C07D333/38 ,  Y02P20/55

摘要： Disclosed is a method of preparing a thiohydrazide product compound from a hydrazide starting compound. The hydrazide starting compound is represented by Structural Formula (I): The thiohydrazide product compound is represented by Structural Formula (II): In Structural Formulas (I)-(II), R1 and R2 are independently an aliphatic group, a substituted aliphatic group, an aryl group or a substituted aryl group, or R1 and R2 taken together with the carbon and nitrogen atoms to which they are bonded, form a non-aromatic heterocyclic ring optionally fused to an aromatic ring. When R2 is an aryl group or a substituted aryl group, then R5 is a hydrazine protecting group; and when R2 is an aliphatic or substituted aliphatic group, then R5 is —H or a hydrazine protecting group. R10 is —H or a substituted or unsubstituted alkyl group. The method comprising the step of reacting the starting compound with a thionylating reagent.

摘要翻译： 公开了从酰肼起始化合物制备硫代酰肼产物化合物的方法。 酰肼起始化合物由结构式（I）表示：硫代酰肼产物化合物由结构式（II）表示：在结构式（I） - （II）中，R 1和R 2独立地为脂族基团，取代的脂族基团 ，芳基或取代的芳基，或者R 1和R 2与它们所键合的碳原子和氮原子一起形成任选地与芳环稠合的非芳族杂环。 当R 2为芳基或取代芳基时，R 5为肼保护基; 当R 2为脂肪族或取代的脂族基团时，R 5为-H或肼保护基。 R 10为-H或取代或未取代的烷基。 该方法包括使起始化合物与亚硫酰化试剂反应的步骤。

公开(公告)号：US06762204B2

公开(公告)日：2004-07-13

申请号：US10193639

申请日：2002-07-10

申请人： Keizo Koya ,  Lijun Sun ,  Shoujun Chen ,  Noriaki Tatsuta ,  Yaming Wu ,  Mitsunori Ono ,  Zhi-Qiang Xia

发明人： Keizo Koya ,  Lijun Sun ,  Shoujun Chen ,  Noriaki Tatsuta ,  Yaming Wu ,  Mitsunori Ono ,  Zhi-Qiang Xia

IPC分类号： A61K3116

CPC分类号： C07D307/68 ,  A45D2008/006 ,  A61K31/337 ,  A61K31/505 ,  A61K31/53 ,  A61K31/5377 ,  A61K47/58 ,  C07C327/56 ,  C07C2601/02 ,  C07C2601/04 ,  C07C2601/08 ,  C07C2601/14 ,  C07D209/42 ,  C07D209/44 ,  C07D213/83 ,  C07D261/18 ,  C07D333/38 ,  C07D333/68

摘要： One embodiment of the present invention is a compound represented by the Structural Formula (I): Y is a covalent bond of a substituted or unsubstituted straight chained hydrocarbyl group. In addition, Y, taken together with both >C═Z groups to which it is bonded, is a substituted or unsubstituted aromatic group. Preferably, Y is a covalent bond or —C(R7R8)—. R1 is an aliphatic group, a substituted aliphatic group, a non-aromatic heterocyclic group, or a substituted non-aromatic heterocyclic group, R2-R4 are independently —H, an aliphatic group, a substituted aliphatic group, a non-aromatic heterocyclic group, a substituted non-aromatic heterocyclic group, an aryl group or a substituted aryl group, or R1 and R3 taken together with the carbon and nitrogen atoms to which they are bonded, and/or R2 and R4 taken together with the carbon and nitrogen atoms to which they are bonded, form a non-aromatic heterocyclic ring optionally fused to an aromatic ring. R5-R6 are independently —H, an aliphatic group, a substituted aliphatic group, an aryl group or a substituted aryl group. R7 and R8 are each independently —H, an aliphatic or substituted aliphatic group, or R7 is —H and R8 is a substituted or unsubstituted aryl group, or, R7 and R8, taken together, are a C2-C6 substituted or unsubstituted alkylene group. Z is ═O or ═S. Also disclosed are pharmaceutical compositions comprising the compound of the present invention and a pharmaceutically acceptable carrier or diluent.

摘要翻译： 本发明的一个实施方案是由结构式（I）表示的化合物：Y是取代或未取代的直链烃基的共价键。 此外，Y与它所键合的两个> C = Z基团一起是取代或未取代的芳族基团。 优选Y为共价键或-C（R7R8） - ，R1为脂肪族基团，取代脂肪族基团，非芳族杂环基团或取代的非芳香族杂环基团，R2-R4独立地为-H， 脂肪族基团，取代脂肪族基团，非芳族杂环基团，取代的非芳族杂环基团，芳基或取代的芳基，或者R 1和R 3与它们所键合的碳原子和氮原子一起 ，和/或R 2和R 4与它们所键合的碳原子和氮原子一起形成任选地与芳环稠合的非芳族杂环.R 5 -R 6独立地是-H，脂族基团，取代的脂族基 基团，芳基或取代的芳基.R 7和R 8各自独立地为-H，脂族或取代的脂族基团，或者R 7为-H且R 8为取代或未取代的芳基，或者R 7和R 8一起 是C2-C6取代或未取代的亚烷基gr 此外，还公开了包含本发明化合物和药学上可接受的载体或稀释剂的药物组合物。

公开(公告)号：US07001923B2

公开(公告)日：2006-02-21

申请号：US10803798

申请日：2004-03-18

申请人： Keizo Koya ,  Lijun Sun ,  Shoujun Chen ,  Noriaki Tatsuta ,  Yaming Wu ,  Mitsunori Ono ,  Zhi-Qiang Xia

发明人： Keizo Koya ,  Lijun Sun ,  Shoujun Chen ,  Noriaki Tatsuta ,  Yaming Wu ,  Mitsunori Ono ,  Zhi-Qiang Xia

IPC分类号： A61K31/16 ,  A61K31/335 ,  C07C327/00 ,  C07D305/00

CPC分类号： C07D307/68 ,  A45D2008/006 ,  A61K31/337 ,  A61K31/505 ,  A61K31/53 ,  A61K31/5377 ,  A61K47/58 ,  C07C327/56 ,  C07C2601/02 ,  C07C2601/04 ,  C07C2601/08 ,  C07C2601/14 ,  C07D209/42 ,  C07D209/44 ,  C07D213/83 ,  C07D261/18 ,  C07D333/38 ,  C07D333/68

摘要： One embodiment of the present invention is a compound represented by the Structural Formula (I): Y is a covalent bond of a substituted or unsubstituted straight chained hydrocarbyl group. In addition, Y, taken together with both >C=Z groups to which it is bonded, is a substituted or unsubstituted aromatic group. Preferably, Y is a covalent bond or —C(R7R8)—.R1 is an aliphatic group, a substituted aliphatic group, a non-aromatic hetereocyclic group, or a substituted non-aromatic hetereocyclic group, R2–R4 are independently —H, an aliphatic group, a substituted aliphatic group, a non-aromatic hetereocyclic group, a substituted non-aromatic hetereocyclic group, an aryl group or a substituted aryl group, or R1 and R3 taken together with the carbon and nitrogen atoms to which they are bonded, and/or R2 and R4 taken together with the carbon and nitrogen atoms to which they are bonded, form a non-aromatic heterocyclic ring optionally fused to an aromatic ring.R5–R6 are independently —H, an aliphatic group, a substituted aliphatic group, an aryl group or a substituted aryl group.R7 and R8 are each independently —H, an aliphatic or substituted aliphatic group, or R7 is —H and R8 is a substituted or unsubstituted aryl group, or, R7 and R8, taken together, are a C2–C6 substituted or unsubstituted alkylene group.Z is ═O or ═S.Also disclosed are pharmaceutical compositions comprising the compound of the present invention and a pharmaceutically acceptable carrier or diluent.

摘要翻译： 本发明的一个实施方案是由结构式（I）表示的化合物：<化学式id =“CHEM-US-00001”num =“000