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1. 发明授权

US08183273B2 Bicyclic compound, production and use thereof 有权
标题翻译：双环化合物，其生产和使用
公开(公告)号：US08183273B2
公开(公告)日：2012-05-22
申请号：US11978198
申请日：2007-10-25
申请人： Mitsuru Shiraishi , Masanori Baba , Katsuji Aikawa , Naoyuki Kanzaki , Masaki Seto , Yuji Iizawa
发明人： Mitsuru Shiraishi , Masanori Baba , Katsuji Aikawa , Naoyuki Kanzaki , Masaki Seto , Yuji Iizawa
IPC分类号： A61P31/18 , A61K31/41 , A61K31/415 , A61K31/35 , C07D487/00
CPC分类号： A61K31/4196 , A61K31/395 , A61K31/4178 , C07D225/06 , C07D313/20 , C07D403/12 , C07D405/12 , C07D407/12
摘要： The present invention provides a new cyclic compound having a CCR antagonist activity, especially a CCR5 antagonist activity, and the use thereof. The compound of the present invention is represented by the formula: wherein, R1 is a 5- to 6-membered ring group which may be substituted; X1 is a bond or the like; ring A is a 5- to 6-membered ring group which may be substituted; ring B is a 8- to 10-membered ring group which may be substituted; X2 is a bivalent group of 1 to 4 atoms; Z1 is a bivalent cyclic ring group or the like; Z2 is a bond or the like; and R2 is an amino group, a nitrogen-containing heterocyclic group which may be substituted or the like, or a salt thereof.
摘要翻译：本发明提供具有CCR拮抗剂活性，特别是CCR5拮抗剂活性的新的环状化合物及其用途。本发明化合物由下式表示：其中，R 1为可被取代的5-至6-元环基; X1是债券等; 环A是可以被取代的5至6元环基团; 环B是可以被取代的8至10元环基团; X 2是1至4个原子的二价基团; Z1是二价环状环基等; Z2是键或类似物; R 2为氨基，可以被取代的含氮杂环基等，或其盐。

2. 发明申请

US20090030032A1 Bicyclic Compound, Production and Use Thereof 有权
标题翻译：双环化合物，其生产和使用
公开(公告)号：US20090030032A1
公开(公告)日：2009-01-29
申请号：US12119355
申请日：2008-05-12
申请人： Mitsuru Shiraishi , Masanori Baba , Katsuji Aikawa , Naoyuki Kanzaki , Masaki Seto , Yuji Iizawa
发明人： Mitsuru Shiraishi , Masanori Baba , Katsuji Aikawa , Naoyuki Kanzaki , Masaki Seto , Yuji Iizawa
IPC分类号： A61K31/44 , C07D401/02
CPC分类号： A61K31/4196 , A61K31/395 , A61K31/4178 , C07D225/06 , C07D313/20 , C07D403/12 , C07D405/12 , C07D407/12
摘要： The present invention provides a new cyclic compound having a CCR antagonist activity, especially a CCR5 antagonist activity, and the use thereof. The compound of the present invention is represented by the formula: wherein, R1 is a 5- to 6-membered ring group which may be substituted; X1 is a bond or the like; ring A is a 5- to 6-membered ring group which may be substituted; ring B is a 8- to 10-membered ring group which may be substituted; X2 is a bivalent group of 1 to 4 atoms; Z1 is a bivalent cyclic ring group or the like; Z2 is a bond or the like; and R2 is an amino group, a nitrogen-containing heterocyclic group which may be substituted or the like, or a salt thereof.
摘要翻译：本发明提供具有CCR拮抗剂活性，特别是CCR5拮抗剂活性的新的环状化合物及其用途。本发明化合物由下式表示：其中，R 1为可被取代的5-至6-元环基; X1是债券等; 环A是可以被取代的5至6元环基团; 环B是可以被取代的8至10元环基团; X 2是1至4个原子的二价基团; Z1是二价环状环基等; Z2是键或类似物; R 2为氨基，可以被取代的含氮杂环基等，或其盐。

3. 发明授权

US08362058B2 Bicyclic compound, production and use thereof 有权
标题翻译：双环化合物，其生产和使用
公开(公告)号：US08362058B2
公开(公告)日：2013-01-29
申请号：US12119355
申请日：2008-05-12
申请人： Mitsuru Shiraishi , Masanori Baba , Katsuji Aikawa , Naoyuki Kanzaki , Masaki Seto , Yuji Iizawa
发明人： Mitsuru Shiraishi , Masanori Baba , Katsuji Aikawa , Naoyuki Kanzaki , Masaki Seto , Yuji Iizawa
IPC分类号： A61P31/18 , A61K31/41 , A61K31/415 , A61K31/35 , C07D487/00
CPC分类号： A61K31/4196 , A61K31/395 , A61K31/4178 , C07D225/06 , C07D313/20 , C07D403/12 , C07D405/12 , C07D407/12
摘要： The present invention provides a new cyclic compound having a CCR antagonist activity, especially a CCR5 antagonist activity, and the use thereof. The compound of the present invention is represented by the formula: wherein, R1 is a 5- to 6-membered ring group which may be substituted; X1 is a bond or the like; ring A is a 5- to 6-membered ring group which may be substituted; ring B is a 8- to 10-membered ring group which may be substituted; X2 is a bivalent group of 1 to 4 atoms; Z1 is a bivalent cyclic ring group or the like; Z2 is a bond or the like; and R2 is an amino group, a nitrogen-containing heterocyclic group which may be substituted or the like, or a salt thereof.
摘要翻译：本发明提供具有CCR拮抗剂活性，特别是CCR5拮抗剂活性的新的环状化合物及其用途。本发明化合物由下式表示：其中，R 1为可被取代的5-至6-元环基; X1是债券等; 环A是可以被取代的5至6元环基团; 环B是可以被取代的8至10元环基团; X 2是1至4个原子的二价基团; Z1是二价环状环基等; Z2是键或类似物; R 2为氨基，可以被取代的含氮杂环基等，或其盐。

4. 发明申请

US20120232028A1 Bicyclic Compound, Production and Use Thereof 有权
标题翻译：双环化合物，其生产和使用
公开(公告)号：US20120232028A1
公开(公告)日：2012-09-13
申请号：US13476454
申请日：2012-05-21
申请人： Mitsuru SHIRAISHI , Masanori BABA , Katsuji AIKAWA , Naoyuki KANZAKI , Masaki SETO , Yuji IIZAWA
发明人： Mitsuru SHIRAISHI , Masanori BABA , Katsuji AIKAWA , Naoyuki KANZAKI , Masaki SETO , Yuji IIZAWA
IPC分类号： A61K31/395 , A61K31/341 , C07D405/12 , A61K31/4178 , C07D403/12 , C07D405/14 , C07D403/14 , A61K31/4196 , C07D225/06 , C07D313/20 , A61K31/7072 , A61K31/708 , A61K31/7068 , A61K31/513 , A61K31/551 , A61K31/496 , A61K31/52 , A61K31/536 , A61K31/427 , A61K31/4725 , C12N5/071 , A61K31/472 , A61P31/18 , A61P29/00 , A61P19/02 , A61P37/06 , A61P37/08 , A61P9/10 , A61P25/00 , A61P13/12 , A01N1/02 , C07D407/12
CPC分类号： A61K31/4196 , A61K31/395 , A61K31/4178 , C07D225/06 , C07D313/20 , C07D403/12 , C07D405/12 , C07D407/12
摘要： The present invention provides a new cyclic compound having a CCR antagonist activity, especially a CCR5 antagonist activity, and the use thereof. The compound of the present invention is represented by the formula: wherein, R1 is a 5- to 6-membered ring group which may be substituted; X1 is a bond or the like; ring A is a 5- to 6-membered ring group which may be substituted; ring B is a 8- to 10-membered ring group which may be substituted; X2 is a bivalent group of 1 to 4 atoms; Z1 is a bivalent cyclic ring group or the like; Z2 is a bond or the like; and R2 is an amino group, a nitrogen-containing heterocyclic group which may be substituted or the like, or a salt thereof.
摘要翻译：本发明提供具有CCR拮抗剂活性，特别是CCR5拮抗剂活性的新的环状化合物及其用途。本发明化合物由下式表示：其中，R 1为可被取代的5-至6-元环基; X1是债券等; 环A是可以被取代的5至6元环基团; 环B是可以被取代的8至10元环基团; X 2是1至4个原子的二价基团; Z1是二价环状环基等; Z2是键或类似物; R 2为氨基，可以被取代的含氮杂环基等，或其盐。

5. 发明申请

US20080161287A1 Bicyclic compound, production and use thereof 有权
标题翻译：双环化合物，其生产和使用
公开(公告)号：US20080161287A1
公开(公告)日：2008-07-03
申请号：US11978198
申请日：2007-10-25
申请人： Mitsuru Shiraishi , Masanori Baba , Katsuji Aikawa , Naoyuki Kanzaki , Masaki Seto , Yuji Lizawa
发明人： Mitsuru Shiraishi , Masanori Baba , Katsuji Aikawa , Naoyuki Kanzaki , Masaki Seto , Yuji Lizawa
IPC分类号： A61K31/55 , C07D401/02 , A61P31/18 , A61P19/02 , A61P9/00 , A01N1/02
CPC分类号： A61K31/4196 , A61K31/395 , A61K31/4178 , C07D225/06 , C07D313/20 , C07D403/12 , C07D405/12 , C07D407/12
摘要： The present invention provides a new cyclic compound having a CCR antagonist activity, especially a CCR5 antagonist activity, and the use thereof. The compound of the present invention is represented by the formula: wherein, R1 is a 5- to 6-membered ring group which may be substituted; X1 is a bond or the like; ring A is a 5- to 6-membered ring group which may be substituted; ring B is a 8- to 10-membered ring group which may be substituted; X2 is a bivalent group of 1 to 4 atoms; Z1 is a bivalent cyclic ring group or the like; Z2 is a bond or the like; and R2 is an amino group, a nitrogen-containing heterocyclic group which may be substituted or the like, or a salt thereof.
摘要翻译：本发明提供具有CCR拮抗剂活性，特别是CCR5拮抗剂活性的新的环状化合物及其用途。本发明的化合物由下式表示：其中R 1为可被取代的5至6元环基团; X 1是键或类似物; 环A是可以被取代的5至6元环基团; 环B是可以被取代的8至10元环基团; X 2是1至4个原子的二价基团; Z 1是二价环状环基等; Z 2是键或类似物; R 2是氨基，可以被取代的含氮杂环基等，或其盐。

6. 发明授权

US07288654B2 Fused-ring pyridine derivative, process for producing the same, and use 失效
标题翻译：稠环吡啶衍生物，其制备方法及用途
公开(公告)号：US07288654B2
公开(公告)日：2007-10-30
申请号：US10544435
申请日：2004-02-05
申请人： Mitsuru Shiraishi , Katsuji Aikawa , Naoyuki Kanzaki , Masanori Baba
发明人： Mitsuru Shiraishi , Katsuji Aikawa , Naoyuki Kanzaki , Masanori Baba
IPC分类号： C07D471/02
CPC分类号： A61K31/55 , C07D471/04
摘要： The present invention provides a compound represented by the formula: wherein R1 is a 5- or 6-membered ring which may be substituted; R3 is a hydrogen atom, a lower alkyl group or a lower alkoxy group; Z1 is a 5- or 6-membered aromatic ring; Z2 is a group represented by -Z2a-W2-Z2b wherein Z2a and Z2b are each O, S(O)m (wherein m is 0, 1 or 2), an imino group, or a bond; and W2 is an alkylene chain which may be substituted; n is an integer of 0 to 4; Y is O, S(O)p (wherein p is 0, 1 or 2), CH2 or NR4 (wherein R4 is a hydrogen atom, a hydrocarbon group, a heterocyclic group, or an acyl group); and R2 is (1) an amino group, in which the nitrogen atom is converted to quaternary ammonium or oxide, (2) a nitrogen-containing heterocyclic group which may contain a sulfur atom or an oxygen atom as a ring-constituting atom, in which the nitrogen atom may be converted to a quaternary ammonium or an oxide, and the like, or a salt thereof. The compound has excellent CCR5 antagonist activity and is useful as a prophylactic and/or therapeutic medicine for HIV infection in human peripheral mononuclear blood cells, especially AIDS.
摘要翻译：本发明提供由下式表示的化合物：其中R 1是可被取代的5或6元环; R 3是氢原子，低级烷基或低级烷氧基; Z 1是5或6元芳环; Z 2是由-Z 2 O 2 -W 2 -Z 2b表示的基团，其中Z 2a （O）m（其中m为0,1或2），亚氨基或键; O，S（O）且W 2是可以被取代的亚烷基链; n为0〜4的整数。 Y是O，S（O）p（其中p是0,1或2），CH 2或NR 4（其中R' SUP> 4 是氢原子，烃基，杂环基或酰基）; 和R 2是（1）氮原子转化为季铵或氧化物的氨基，（2）可含有硫原子或氧原子的含氮杂环基作为其中氮原子可以转化为季铵或氧化物的环构成原子等，或其盐。该化合物具有优异的CCR5拮抗剂活性，可用作人外周血单核细胞尤其是艾滋病中HIV感染的预防和/或治疗药物。

7. 发明授权

US07371772B2 Bicyclic compound, production and use thereof 有权
公开(公告)号：US07371772B2
公开(公告)日：2008-05-13
申请号：US10484762
申请日：2002-08-07
申请人： Mitsuru Shiraishi , Masanori Baba , Katsuji Aikawa , Naoyuki Kanzaki , Masaki Seto , Yuji Iizawa
发明人： Mitsuru Shiraishi , Masanori Baba , Katsuji Aikawa , Naoyuki Kanzaki , Masaki Seto , Yuji Iizawa
IPC分类号： A61P31/18 , A61K31/335 , A61K31/395 , A61K31/4178 , A61K31/4196 , C07D313/20 , C07D225/06 , C07D403/12 , C07D405/14 , C07D403/14
CPC分类号： A61K31/4196 , A61K31/395 , A61K31/4178 , C07D225/06 , C07D313/20 , C07D403/12 , C07D405/12 , C07D407/12
摘要： The present invention provides a new cyclic compound having a CCR antagonist activity, especially a CCR5 antagonist activity, and the use thereof. The compound of the present invention is represented by the formula: wherein, R1 is a 5- to 6-membered ring group which may be substituted; X1 is a bond or the like; ring A is a 5- to 6-membered ring group which may be substituted; ring B is a 8- to 10-membered ring group which may be substituted; X2 is a bivalent group of 1 to 4 atoms; Z1 is a bivalent cyclic ring group or the like; Z2 is a bond or the like; and R2 is an amino group, a nitrogen-containing heterocyclic group which may be substituted or the like, or a salt thereof.

8. 发明申请

US20060100197A1 Fused-ring pyridine derivative, process for producing the same, and use 失效
标题翻译：稠环吡啶衍生物，其制备方法及用途
公开(公告)号：US20060100197A1
公开(公告)日：2006-05-11
申请号：US10544435
申请日：2004-02-05
申请人： Mitsuru Shiraishi , Katsuji Aikawa , Naoyuki Kanzaki , Masanori Baba
发明人： Mitsuru Shiraishi , Katsuji Aikawa , Naoyuki Kanzaki , Masanori Baba
IPC分类号： A61K31/55 , A61K31/541 , A61K31/5377 , A61K31/496 , A61K31/4743 , A61K31/4741 , C07D498/02 , C07D491/02 , C07D471/02
CPC分类号： A61K31/55 , C07D471/04
摘要： The present invention provides a compound represented by the formula: wherein R1 is a 5- or 6-membered ring which may be substituted; R3 is a hydrogen atom, a lower alkyl group or a lower alkoxy group; Z1 is a 5- or 6-membered aromatic ring; Z2 is a group represented by -Z2a-W2-Z2b wherein Z2a and Z2b are each O, S(O)m (wherein m is 0, 1 or 2), an imino group, or a bond; and W2 is an alkylene chain which may be substituted; n is an integer of 0 to 4; Y is O, S(O)p (wherein p is 0, 1 or 2), CH2 or NR4 (wherein R4 is a hydrogen atom, a hydrocarbon group, a heterocyclic group, or an acyl group); and R2 is (1) an amino group, in which the nitrogen atom is converted to quaternary ammonium or oxide, (2) a nitrogen-containing heterocyclic group which may contain a sulfur atom or an oxygen atom as a ring-constituting atom, in which the nitrogen atom may be converted to a quaternary ammonium or an oxide, and the like, or a salt thereof. The compound has excellent CCR5 antagonist activity and is useful as a prophylactic and/or therapeutic medicine for HIV infection in human peripheral mononuclear blood cells, especially AIDS.
摘要翻译：本发明提供由下式表示的化合物：其中R 1是可被取代的5或6元环; R 3是氢原子，低级烷基或低级烷氧基; Z 1是5或6元芳环; Z 2是由-Z 2 O 2 -W 2 -Z 2b表示的基团，其中Z 2a （O）m（其中m为0,1或2），亚氨基或键; O，S（O）且W 2是可以被取代的亚烷基链; n为0〜4的整数。 Y是O，S（O）p（其中p是0,1或2），CH 2或NR 4（其中R' SUP> 4 是氢原子，烃基，杂环基或酰基）; 和R 2是（1）氮原子转化为季铵或氧化物的氨基，（2）可含有硫原子或氧原子的含氮杂环基作为其中氮原子可以转化为季铵或氧化物的环构成原子等，或其盐。该化合物具有优异的CCR5拮抗剂活性，可用作人外周血单核细胞尤其是艾滋病中HIV感染的预防和/或治疗药物。

9. 发明申请

US20060160864A1 Acrylamide derivative, process for producing the same, and use 审中-公开
标题翻译：丙烯酰胺衍生物，其制造方法和用途
公开(公告)号：US20060160864A1
公开(公告)日：2006-07-20
申请号：US10544275
申请日：2004-02-02
申请人： Mitsuru Shiraishi , Masaki Seto , Katsuji Aikawa , Naoyuki Kanzaki , Masanori Baba
发明人： Mitsuru Shiraishi , Masaki Seto , Katsuji Aikawa , Naoyuki Kanzaki , Masanori Baba
IPC分类号： A61K31/4439 , A61K31/4178 , A61K31/40 , C07D403/02
CPC分类号： C07D213/73
摘要： A compound represented by the formula: wherein R1 is a 5- or 6-membered ring; R3 is a hydrogen atom, a lower alkyl group or a lower alkoxy group; R7 and R8 are each a hydrogen atom or a lower alkyl group; Z1 is another 5- or 6-membered aromatic ring; Z2 is a group represented by -Z2a-W1-Z2b- [wherein Z2a and Z2b are each O, S(O)m (wherein m is 0, 1 or 2), an imino group or a bond, and W1 is an alkylene chain]; X is CR (wherein R is a hydrogen atom, a lower alkyl group, a lower alkoxy group, an acyl group, or R and adjacent R4 may form a 5- or 6-membered alicyclic heterocyclic group) or N; R4 is NR5R6 (wherein R5 and R6 are each a hydrogen atom, a hydrocarbon group, a heterocyclic group or an acyl group), or R5 and R6 are bonded to each other to form a heterocyclic group of NR5R6; and R2 is (1) an amino group which may be a quaternary ammonium or oxide, (2) a nitrogen-containing heterocyclic group which may contain a sulfur atom or an oxygen atom as the ring-constituting atom, in which the nitrogen atom may be converted to a quaternary ammonium or an oxide, or the like; or a salt thereof. The compound has excellent CCR5 antagonistic activity and thus is useful as a prophylactic and/or therapeutic medicine for HIV infection into human peripheral blood monocyte, especially for AIDS.
摘要翻译：由下式表示的化合物：其中R 1是5或6元环; R 3是氢原子，低级烷基或低级烷氧基; R 7和R 8各自为氢原子或低级烷基; Z 1是另一个5或6元芳环; Z 2是由-Z 2a表示的基团，其中Z ^{2a和Z 2b各自为O，S（O）m（其中m为0,1或2），亚氨基或键，和W 1是亚烷基链]; X是CR（其中R是氢原子，低级烷基，低级烷氧基，酰基或R和相邻的R 4）可以形成5-或6-元脂环族杂环基）或N; R 4是NR 5 R 6（其中R 5和R 6）是各自为氢原子，烃基，杂环基或酰基）或R 5和R 6彼此键合以形成NR的杂环基 5＆lt; 5＆gt; 6＆lt; 6＆gt; 和R 2是（1）可以是季铵或氧化物的氨基，（2）可以含有硫原子或氧原子的含氮杂环基作为环的构成原子，其中氮原子可以转化成季铵或氧化物等; 或其盐。该化合物具有优异的CCR5拮抗活性，因此可用作HIV感染人外周血单核细胞，特别是用于艾滋病的预防和/或治疗药物。}

10. 发明授权

US08741943B2 Bicyclic compound, production and use thereof 有权
标题翻译：双环化合物，其生产和使用
公开(公告)号：US08741943B2
公开(公告)日：2014-06-03
申请号：US13476454
申请日：2012-05-21
申请人： Mitsuru Shiraishi , Masanori Baba , Katsuji Aikawa , Naoyuki Kanzaki , Masaki Seto , Yuji Iizawa
发明人： Mitsuru Shiraishi , Masanori Baba , Katsuji Aikawa , Naoyuki Kanzaki , Masaki Seto , Yuji Iizawa
IPC分类号： C07D403/02 , A61K31/4178
CPC分类号： A61K31/4196 , A61K31/395 , A61K31/4178 , C07D225/06 , C07D313/20 , C07D403/12 , C07D405/12 , C07D407/12
摘要： The present invention provides a new cyclic compound having a CCR antagonist activity, especially a CCR5 antagonist activity, and the use thereof. The compound of the present invention is represented by the formula: wherein, R1 is a 5- to 6-membered ring group which may be substituted; X1 is a bond or the like; ring A is a 5- to 6-membered ring group which may be substituted; ring B is a 8- to 10-membered ring group which may be substituted; X2 is a bivalent group of 1 to 4 atoms; Z1 is a bivalent cyclic ring group or the like; Z2 is a bond or the like; and R2 is an amino group, a nitrogen-containing heterocyclic group which may be substituted or the like, or a salt thereof.
摘要翻译：本发明提供具有CCR拮抗剂活性，特别是CCR5拮抗剂活性的新的环状化合物及其用途。本发明化合物由下式表示：其中，R 1为可被取代的5-至6-元环基; X1是债券等; 环A是可以被取代的5至6元环基团; 环B是可以被取代的8至10元环基团; X 2是1至4个原子的二价基团; Z1是二价环状环基等; Z2是键或类似物; R 2为氨基，可以被取代的含氮杂环基等，或其盐。

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