公开(公告)号：US06750219B1

公开(公告)日：2004-06-15

申请号：US10048914

申请日：2002-02-05

申请人： Keiichi Ajito ,  Naokazu Yahata ,  Minoru Ishikawa ,  Dai Kubota ,  Shoichi Murakami ,  Mikio Yamamoto ,  Kazuyuki Fujishima ,  Shuichi Gomi ,  Shokichi Ouchi

发明人： Keiichi Ajito ,  Naokazu Yahata ,  Minoru Ishikawa ,  Dai Kubota ,  Shoichi Murakami ,  Mikio Yamamoto ,  Kazuyuki Fujishima ,  Shuichi Gomi ,  Shokichi Ouchi

IPC分类号： C07D40304

CPC分类号： C07D239/42

摘要： An objective of the present invention is to provide highly water-soluble compounds having integrin &agr;v&bgr;3 antagonistic activity. The compounds according to the present invention are compounds represented by formula (I) and pharmaceutically acceptable salts or solvates thereof: wherein A represents a two nitrogen atom-containing optionally substituted saturated or unsaturated five- to seven-membered heterocyclic group, which is optionally condensed with another carbocyclic ring or heterocyclic ring to form a bicyclic group, or —C(—NR1R2)(═NR3) wherein R1, R2, and R3 represent hydrogen, alkyl or the like; D represents a bond, >NR4, wherein R4 represents hydrogen or optionally substituted alkyl, —O—, or —S—; X and Z represent either CH or N; R7 and R8 represent C1-6 alkyl, halogen, oxygen or the like; Q represents >C═O, >CHR13 or >CHOR13 wherein R13 represents hydrogen or alkyl; R9 represents hydrogen, alkyl or the like; J represents a bond or alkylene having 1 to 3 carbon atoms; R10 and R11 represent hydrogen, alkyl or the like; m is an integer of 0 to 5; n is an integer of 0 to 4; and p and q are an integer of 1 to 3.

摘要翻译： 本发明的目的是提供具有整合素α2拮抗活性的高水溶性化合物。 根据本发明的化合物是由式（I）表示的化合物及其药学上可接受的盐或溶剂化物：其中A表示两个含有氮原子的任选取代的饱和或不饱和的五至七元杂环基，其任选地稠合 与另一个碳环或杂环形成双环基团，或-C（-NR 1 R 2）（= NR 3）（其中R 1，R 2和R 3） 代表氢，烷基等; D表示键，NR 4，其中R 4表示氢或任选取代的烷基，-O-或-S-; X和Z表示CH或N; R 7和R 8表示C 1-6烷基，卤素，氧等; Q表示C = O，> CHR 13或CHOR 13，其中R 13表示氢或烷基; R 9表示氢，烷基等; J表示碳原子数1〜3的键或亚烷基。 R 10和R 11代表氢，烷基等; m为0〜5的整数。 n为0〜4的整数。 p和q为1〜3的整数。

公开(公告)号：US20050059669A1

公开(公告)日：2005-03-17

申请号：US10944712

申请日：2004-09-21

申请人： Keiichi Ajito ,  Minoru Ishikawa ,  Dai Kubota ,  Shoichi Murakami ,  Mikio Yamamoto ,  Naokazu Yahata ,  Kazuyuki Fujishima ,  Makoto Oyama

发明人： Keiichi Ajito ,  Minoru Ishikawa ,  Dai Kubota ,  Shoichi Murakami ,  Mikio Yamamoto ,  Naokazu Yahata ,  Kazuyuki Fujishima ,  Makoto Oyama

IPC分类号： C07C229/54 ,  C07C229/60 ,  C07D239/14 ,  C07D239/42 ,  C07D401/12 ,  A61K31/496 ,  A61K31/454 ,  C07D43/02

CPC分类号： C04B35/632 ,  C07C229/54 ,  C07C229/60 ,  C07D239/14 ,  C07D239/42 ,  C07D401/12

摘要： An object of the present invention is to provide m-substituted benzoic acid derivatives having integrin αvβ3 antagonistic activity. The derivatives according to the present invention are compounds represented by formula (I) or pharmaceutically acceptable salts or solvates thereof, which are useful for the treatment or prevention of cardiovascular diseases, angiogenesis-related diseases, cerebrovascular diseases, cancers and metastasis thereof, immunological diseases, osteopathy and other diseases: wherein A represents an optionally substituted heterocyclic group containing two nitrogen atoms, a bicylic group or the like; D represents a bond, >NR4, >CR5R6, O, S, or —NR4—CR5R6—; X represents CH or N; R7 and R8 represent hydroxyl, alkyl or the like; Q represents >C═O or the like; R9 represents hydrogen, alkyl or the like; J represents a bond or alkylene; R10 represents optionally substituted hydroxyl, amino or the like; R11 represents hydrogen, alkyl or the like; m is 0 to 5; n is 0 to 4; and p and q are each 0 to 3.

摘要翻译： 本发明的目的是提供具有整合素α噬菌体拮抗活性的m取代苯甲酸衍生物。 根据本发明的衍生物是由式（I）表示的化合物或其药学上可接受的盐或溶剂化物，其可用于治疗或预防心血管疾病，血管生成相关疾病，脑血管疾病，癌症及其转移，免疫疾病 ，骨病和其他疾病：其中A表示任选取代的含有两个氮原子的杂环基团，二等基团等; D表示键，NR 4，CR 5 R 6，O，S或-NR 4 -CR 5 R 6 - 。 X表示CH或N; R 7和R 8代表羟基，烷基等; Q表示> C = O等; R 9表示氢，烷基等; J表示键或亚烷基; R 10表示任选取代的羟基，氨基等; R 11表示氢，烷基等; m为0〜5; n为0〜4; p和q各自为0〜3。

公开(公告)号：US06451800B1

公开(公告)日：2002-09-17

申请号：US09601176

申请日：2000-07-28

申请人： Keiichi Ajito ,  Shoichi Murakami ,  Minoru Ishikawa ,  Mikio Yamamoto ,  Dai Kubota ,  Shuichi Gomi ,  Mitsugu Hachisu ,  Kiyoaki Katano

发明人： Keiichi Ajito ,  Shoichi Murakami ,  Minoru Ishikawa ,  Mikio Yamamoto ,  Dai Kubota ,  Shuichi Gomi ,  Mitsugu Hachisu ,  Kiyoaki Katano

IPC分类号： A61K31497

CPC分类号： C07D239/42 ,  C07D235/30 ,  C07D239/14

摘要： An objective of the present invention is to provide compounds having integrin &agr;v&bgr;3 antagonistic activity, GP IIb/IIIa antagonistic activity, and/or human platelet aggregation inhibitory activity, and therapeutic agents for treating integrin &agr;v&bgr;3-mediated diseases and for inhibiting platelet aggregation. The derivatives according to the present invention are compounds represented by formula (I) or pharmaceutically acceptable salts or solvates thereof: wherein A represents a five- to seven-membered heterocyclic ring containing two nitrogen atoms or the like; X and Z represent CH or a nitrogen atom; R4 and R5 represent alkyl, halogen or the like; Q represents >C=O, >CH2 or the like; R6 represents H, alkyl, aralkyl or the like; R7 represents H, alkynyl or the like; R8 represents H, substituted amino or the like; R9 represents H or alkyl; m is 0 to 5; n is 0 to 4; p is 2 or 3; and q is 0 or 1.

摘要翻译： 本发明的目的是提供具有整合素α2拮抗活性，GP IIb / IIIa拮抗活性和/或人血小板聚集抑制活性的化合物，以及用于治疗整合素α1β介导的疾病和抑制血小板聚集的治疗剂。 根据本发明的衍生物是由式（I）表示的化合物或其药学上可接受的盐或溶剂化物：其中A表示含有两个氮原子等的5-至7-元杂环; X和Z表示CH或氮原子; R4和R5代表烷基，卤素等; Q表示> C = O，> CH2等; R6表示H，烷基，芳烷基等; R 7表示H，炔基等; R8表示H，取代的氨基等; R9代表H或烷基; m为0〜5; n为0〜4; p为2或3; q为0或1。

公开(公告)号：US06420558B1

公开(公告)日：2002-07-16

申请号：US09673017

申请日：2000-10-10

申请人： Minoru Ishikawa ,  Shoichi Murakami ,  Mikio Yamamoto ,  Dai Kubota ,  Mitsugu Hachisu ,  Kiyoaki Katano ,  Keiichi Ajito

发明人： Minoru Ishikawa ,  Shoichi Murakami ,  Mikio Yamamoto ,  Dai Kubota ,  Mitsugu Hachisu ,  Kiyoaki Katano ,  Keiichi Ajito

IPC分类号： C07D23902

CPC分类号： C07D235/14 ,  C07D401/12

摘要： An objective of the present invention is to provide compounds having integrin &agr;v&bgr;3 antagonistic activity, cell adhesion inhibitory activity, GP IIb/IIIa antagonistic activity, and/or human platelet aggregation inhibitory activity, and, therapeutic agents for treating cardiovascular diseases, angiogenesis-related diseases, cerebrovascular diseases and the like and for inhibiting platelet aggregation. The derivatives according to the present invention are compounds represented by formula (I) or pharmaceutically acceptable salts or solvates thereof: wherein A represents a five- to seven-membered heterocyclic group containing two nitrogen atoms or the like; D represents >NH2, >CH2 or the like; X and Z represent CH or a nitrogen atom; R7 and R8 represent alkyl, halogen or the like; Q represents >C═O, >CH2 or the like; R9 represents H, alkyl, aralkyl or the like; R10 represents H, alkynyl or the like; R11 represents H, substituted amino or the like; R12 represents H or alkyl; m is 0 to 5; n is 0 to 4; p and q are each 1 to 3; and r is 0 or 1.

摘要翻译： 本发明的目的是提供具有整合素α噬菌体拮抗活性，细胞粘附抑制活性，GP IIb / IIIa拮抗活性和/或人血小板聚集抑制活性的化合物，以及用于治疗心血管疾病，血管发生相关疾病 脑血管疾病等，并用于抑制血小板聚集。 根据本发明的衍生物是由式（I）表示的化合物或其药学上可接受的盐或溶剂合物：其中A表示含有两个氮原子等的5-至7-元杂环基; D表示> NH 2，> CH 2等; X和Z表示CH或氮原子; R 7和R 8表示烷基，卤素等; Q表示> C = O，> CH2等; R 9表示H，烷基，芳烷基等; R 10表示H，炔基等; R11表示H，取代的氨基等; R 12表示H或烷基; m为0〜5; n为0〜4; p和q各自为1至3; r为0或1。

公开(公告)号：US07871982B2

公开(公告)日：2011-01-18

申请号：US12086279

申请日：2006-12-11

申请人： Eijirou Umemura ,  Yoshinari Wakiyama ,  Kazutaka Ueda ,  Kou Kumura ,  Satomi Masaki ,  Takashi Watanabe ,  Mikio Yamamoto ,  Chizuko Kaji ,  Keiichi Ajito

发明人： Eijirou Umemura ,  Yoshinari Wakiyama ,  Kazutaka Ueda ,  Kou Kumura ,  Satomi Masaki ,  Takashi Watanabe ,  Mikio Yamamoto ,  Chizuko Kaji ,  Keiichi Ajito

IPC分类号： A01N43/04 ,  A61K31/70 ,  C07H15/16

CPC分类号： C07H15/16

摘要： This invention provides compounds of formula (I) or its pharmacologically acceptable salt or solvate, wherein A represents aryl or a monocyclic or bicyclic heterocyclic group, R1 represents a halide, nitro, substituted C1-6 alkyl, optionally substituted amino, C1-6 alkyloxycarbonyl, optionally substituted aryl, a heterocyclic group, or heterocyclic carbonyl, R2 represents a hydrogen atom or C1-6 alkyl, R3 represents C1-6 alkyl, all of R4, R5, and R6 represent a hydrogen atom, R7 represents C1-6 alkyl, m is 1 or 2, and n is 1. The compounds are novel lincomycin derivatives having a potent activity against resistant pneumococci. The compounds can be used as an antimicrobial agent and are useful for preventing or treating bacterial infectious diseases.

摘要翻译： 本发明提供式（I）化合物或其药理学上可接受的盐或溶剂合物，其中A表示芳基或单环或双环杂环基，R 1表示卤素，硝基，取代的C 1-6烷基，任选取代的氨基，C 1-6烷氧基羰基 ，任选取代的芳基，杂环基或杂环羰基，R 2表示氢原子或C 1-6烷基，R 3表示C 1-6烷基，所有R 4，R 5和R 6表示氢原子，R 7表示C 1-6烷基 ，m为1或2，n为1.该化合物是对耐药性肺炎球菌有强力活性的新型林可霉素衍生物。 该化合物可用作抗微生物剂并且可用于预防或治疗细菌感染性疾病。

公开(公告)号：US20100184746A1

公开(公告)日：2010-07-22

申请号：US12451752

申请日：2008-05-30

申请人： Eijirou Umemura ,  Kou Kumura ,  Satomi Masaki ,  Kazutaka Ueda ,  Yoshinari Wakiyama ,  Yasuo Sato ,  Mikio Yamamoto ,  Keiichi Ajito ,  Takashi Watanabe ,  Chizuko Kaji

发明人： Eijirou Umemura ,  Kou Kumura ,  Satomi Masaki ,  Kazutaka Ueda ,  Yoshinari Wakiyama ,  Yasuo Sato ,  Mikio Yamamoto ,  Keiichi Ajito ,  Takashi Watanabe ,  Chizuko Kaji

IPC分类号： A61K31/55 ,  C07D405/14 ,  A61K31/506 ,  C07D405/02 ,  A61K31/4025 ,  C07D401/02 ,  A61K31/4439 ,  C07D285/12 ,  A61K31/433 ,  C07D413/14 ,  A61K31/422 ,  A61K31/501 ,  A61K31/496 ,  A61K31/5377 ,  A61P31/04 ,  A61P11/00

CPC分类号： C07H15/16

摘要： An objective of the present invention is to provide compounds of formula (I) or their pharmacologically acceptable salts or solvates wherein A represents aryl while R1 represents a five- or six-membered monocyclic heterocyclic group, or A represents a four- to six-membered monocyclic heterocyclic group while R1 represents aryl or a five- or six-membered monocyclic heterocyclic group; R2 represents a hydrogen atom or C1-6 alkyl; R3 represents C1-6 alkyl or C3-6 cycloalkyl-C1-4 alkyl; R4, R5, and R6 represent a hydrogen atom; R7 represents C1-6 alkyl; and m is 1 to 3. The compounds are novel lincosamide derivatives that have a potent activity against resistant Streptococcus pneumoniae. Further, the compounds are usable as antimicrobial agents and are useful for preventing or treating bacterial infectious diseases.

摘要翻译： 本发明的目的是提供式（I）化合物或其药理学上可接受的盐或溶剂化物，其中A表示芳基，而R1表示五元或六元单环杂环基，或A表示四至六元 单环杂环基，而R1代表芳基或五元或六元单环杂环基; R2表示氢原子或C1-6烷基; R 3表示C 1-6烷基或C 3-6环烷基-C 1-4烷基; R4，R5和R6表示氢原子; R 7表示C 1-6烷基; 并且m为1至3.该化合物是对耐药性肺炎链球菌具有有效活性的新型长春花胺衍生物。 此外，该化合物可用作抗微生物剂，并且可用于预防或治疗细菌感染性疾病。

公开(公告)号：US07867980B2

公开(公告)日：2011-01-11

申请号：US12451752

申请日：2008-05-30

申请人： Eijirou Umemura ,  Kou Kumura ,  Satomi Masaki ,  Kazutaka Ueda ,  Yoshinari Wakiyama ,  Yasuo Sato ,  Mikio Yamamoto ,  Keiichi Ajito ,  Takashi Watanabe ,  Chizuko Kaji

发明人： Eijirou Umemura ,  Kou Kumura ,  Satomi Masaki ,  Kazutaka Ueda ,  Yoshinari Wakiyama ,  Yasuo Sato ,  Mikio Yamamoto ,  Keiichi Ajito ,  Takashi Watanabe ,  Chizuko Kaji

IPC分类号： A01N43/04 ,  A61K31/70 ,  C07H15/16

CPC分类号： C07H15/16

摘要： An objective of the present invention is to provide compounds of formula (I) or their pharmacologically acceptable salts or solvates wherein A represents aryl while R1 represents a five- or six-membered monocyclic heterocyclic group, or A represents a four- to six-membered monocyclic heterocyclic group while R1 represents aryl or a five- or six-membered monocyclic heterocyclic group; R2 represents a hydrogen atom or C1-6 alkyl; R3 represents C1-6 alkyl or C3-6 cycloalkyl-C1-4 alkyl; R4, R5, and R6 represent a hydrogen atom; R7 represents C1-6 alkyl; and m is 1 to 3. The compounds are novel lincosamide derivatives that have a potent activity against resistant Streptococcus pneumoniae. Further, the compounds are usable as antimicrobial agents and are useful for preventing or treating bacterial infectious diseases.

摘要翻译： 本发明的目的是提供式（I）化合物或其药理学上可接受的盐或溶剂化物，其中A表示芳基，而R1表示五元或六元单环杂环基，或A表示四至六元 单环杂环基，而R1代表芳基或五元或六元单环杂环基; R2表示氢原子或C1-6烷基; R 3表示C 1-6烷基或C 3-6环烷基-C 1-4烷基; R4，R5和R6表示氢原子; R 7表示C 1-6烷基; 并且m为1至3.该化合物是对耐药性肺炎链球菌具有有效活性的新型长春花胺衍生物。 此外，该化合物可用作抗微生物剂，并且可用于预防或治疗细菌感染性疾病。

公开(公告)号：US20090156512A1

公开(公告)日：2009-06-18

申请号：US12086279

申请日：2006-12-11

申请人： Eijirou Umemura ,  Yoshinari Wakiyama ,  Kazutaka Ueda ,  Kou Kumura ,  Satomi Masaki ,  Takashi Watanabe ,  Mikio Yamamoto ,  Chizuko Kaji ,  Keiichi Ajito

发明人： Eijirou Umemura ,  Yoshinari Wakiyama ,  Kazutaka Ueda ,  Kou Kumura ,  Satomi Masaki ,  Takashi Watanabe ,  Mikio Yamamoto ,  Chizuko Kaji ,  Keiichi Ajito

IPC分类号： A61K31/7004 ,  C07H15/16 ,  A61P31/04

CPC分类号： C07H15/16

摘要： This invention provides compounds of formula (I) or its pharmacologically acceptable salt or solvate, wherein A represents aryl or a monocyclic or bicyclic heterocyclic group, R1 represents a halide, nitro, substituted C1-6 alkyl, optionally substituted amino, C1-6 alkyloxycarbonyl, optionally substituted aryl, a heterocyclic group, or heterocyclic carbonyl, R2 represents a hydrogen atom or C1-6 alkyl, R3 represents C1-6 alkyl, all of R4, R5, and R6 represent a hydrogen atom, R7 represents C1-6 alkyl, m is 1 or 2, and n is 1. The compounds are novel lincomycin derivatives having a potent activity against resistant pneumococci. The compounds can be used as an antimicrobial agent and are useful for preventing or treating bacterial infectious diseases.

摘要翻译： 本发明提供式（I）化合物或其药理学上可接受的盐或溶剂合物，其中A表示芳基或单环或双环杂环基，R 1表示卤素，硝基，取代的C 1-6烷基，任选取代的氨基，C 1-6烷氧基羰基 ，任选取代的芳基，杂环基或杂环羰基，R 2表示氢原子或C 1-6烷基，R 3表示C 1-6烷基，所有R 4，R 5和R 6表示氢原子，R 7表示C 1-6烷基 ，m为1或2，n为1.该化合物是对耐药性肺炎球菌有强力活性的新型林可霉素衍生物。 该化合物可用作抗微生物剂并且可用于预防或治疗细菌感染性疾病。

公开(公告)号：US08538245B2

公开(公告)日：2013-09-17

申请号：US12214464

申请日：2008-06-19

申请人： Mikio Yamamoto

发明人： Mikio Yamamoto

IPC分类号： H04N5/76

CPC分类号： H04N5/782 ,  H04N5/775 ,  H04N21/4334 ,  H04N21/43615 ,  H04N21/44231 ,  H04N21/47214

摘要： A recording control apparatus includes the following elements. A receiving unit is configured to receive, from each of a plurality of recording apparatuses, recording schedule information set on a recording apparatus and available-recording-capacity information of the recording apparatus. A determination unit is configured to determine a program to be recorded. A control unit is configured to perform control to select one of the recording apparatuses on the basis of the recording schedule information and the available-recording-capacity information received from the plurality of recording apparatuses and to transmit, to the selected recording apparatus, information for scheduling the recording of the determined program.

公开(公告)号：US07828281B2

公开(公告)日：2010-11-09

申请号：US12042480

申请日：2008-03-05

申请人： Yasunobu Terao ,  Mikio Yamamoto

发明人： Yasunobu Terao ,  Mikio Yamamoto

IPC分类号： B65H29/46

CPC分类号： B65H29/52 ,  B65H2407/10 ,  B65H2511/152 ,  B65H2511/20 ,  B65H2511/415 ,  B65H2801/27 ,  B65H2220/01 ,  B65H2220/02

摘要： When a sheet is conveyed from a processing tray to a stacking tray, a bar-like pushing member is moved in a direction of the stacking tray in synchronization with an ejector. Consequently, simultaneously with the movement of the sheet by the ejector, a lower surface of a leading end of the sheet is pushed to relax and reduce a contact force between the lower surface of the leading end of the sheet and the stacking tray (or an upper surface of a sheet already stacked on the stacking tray). As a result, static friction at the leading end of the sheet is changed to dynamic friction and the entire sheet is conveyed to the stacking tray without bending.

摘要翻译： 当片材从处理托盘输送到堆叠托盘时，条形推动构件与排出器同步地沿着堆叠托盘的方向移动。 因此，与片材由喷射器的移动同时，片材的前端的下表面被推动以松弛并减小片材的前端的下表面与堆垛托盘之间的接触力（或者 已经堆叠在堆垛盘上的纸张的上表面）。 结果，片材前端的静摩擦变为动摩擦，整个片材都没有弯曲地传送到堆垛盘。