公开(公告)号：US5877318A

公开(公告)日：1999-03-02

申请号：US113826

申请日：1998-07-10

申请人： Yoshiaki Isobe ,  Yuso Goto ,  Masanori Tobe ,  Osamu Takahashi

发明人： Yoshiaki Isobe ,  Yuso Goto ,  Masanori Tobe ,  Osamu Takahashi

IPC分类号： C07D239/54 ,  C07D239/545 ,  C07D405/12

CPC分类号： C07D239/545 ,  C07D405/12

摘要： Disclosed is a hydroquinone derivative or a pharmaceutically acceptable salt thereof, the hydroquinone derivative being represented by formula (I): ##STR1## wherein R.sup.1 is a phenyl group which is unsubstituted or substituted with a substituent or substituents each independently selected from the group consisting of a halogen atom, a C1-4 alkyl group and a C1-4 alkoxy group;R.sup.2 is a hydrogen atom or a C1-4 alkyl group;each of R.sup.3 and R.sup.4 is independently a hydrogen atom or a C1-4 alkyl group;R.sup.5 is a hydrogen atom or a C1-4 alkyl group;each of R.sup.6, R.sup.7 and R.sup.8 is independently a hydrogen atom or a C1-4 alkyl group;P is a hydroxyl group;Q is a hydroxyl group, a C1-4 alkoxy group, a C1-18 acyloxy group or an oxo group;P may form together with Q an ether bond;R is a hydroxyl group, a C1-4 alkoxy group, a C1-18 acyloxy group or an oxo group, provided that when one of said Q and said R is an oxo group, the other is also an oxo group;X is a single bond, an --NR.sup.10 -- group or a --CH.sub.2 --NR.sup.10 -- group in which R.sup.10 is a hydrogen atom or a C1-4 alkyl group;Y is a methylene group or a carbonyl group; anddotted bonds in a six membered ring represent that said six membered ring has the maximum number of double bonds.

摘要翻译： 公开了氢醌衍生物或其药学上可接受的盐，氢醌衍生物由式（I）表示：未取代或被各自独立地选自卤素原子，C 1-4烷基的取代基或取代基取代 和C 1-4烷氧基; R2是氢原子或C1-4烷基; R 3和R 4各自独立地为氢原子或C 1-4烷基; R5是氢原子或C1-4烷基; R6，R7和R8各自独立地为氢原子或C1-4烷基; P是羟基; Q是羟基，C 1-4烷氧基，C 1-18酰氧基或氧代基; P可与Q形成醚键; R是羟基，C 1-4烷氧基，C 1-18酰氧基或氧代基，条件是当所述Q和所述R中的一个是氧代基时，另一个也是氧代基; X是单键，-NR 10 - 基或-CH 2 -NR 10 - 基，其中R 10是氢原子或C 1-4烷基; Y是亚甲基或羰基; 六元环中的点状键表示所述六元环具有最大数量的双键。

公开(公告)号：US5821247A

公开(公告)日：1998-10-13

申请号：US933208

申请日：1997-09-16

申请人： Yoshiaki Isobe ,  Yuso Goto ,  Masanori Tobe ,  Osamu Takahashi

发明人： Yoshiaki Isobe ,  Yuso Goto ,  Masanori Tobe ,  Osamu Takahashi

IPC分类号： C07D239/54 ,  C07D239/545 ,  C07D405/12 ,  A61K31/51

CPC分类号： C07D239/545 ,  C07D405/12

摘要： Disclosed is a hydroquinone derivative or a pharmaceutically acceptable salt thereof, the hydroquinone derivative being represented by formula (I): ##STR1## wherein R.sup.1 is a phenyl group which is unsubstituted or substituted with a substituent or substituents each independently selected from the group consisting of a halogen atom, a C1-4 alkyl group and a C1-4 alkoxy group; R.sup.2 is a hydrogen atom or a C1-4 alkyl group; each of R.sup.3 and R.sup.4 is independently a hydrogen atom or a C1-4 alkyl group; R.sup.5 is a hydrogen atom or a C1-4 alkyl group; each of R.sup.6, R.sup.7 and R.sup.8 is independently a hydrogen atom or a C1-4 alkyl group; P is a hydroxyl group; Q is a hydroxyl group, a C1-4 alkoxy group, a C1-18 acyloxy group or an oxo group; P may form together with Q an ether bond; R is a hydroxyl group, a C1-4 alkoxy group, a C1-18 acyloxy group or an oxo group, provided that when one of said Q and said R is an oxo group, the other is also an oxo group; X is a single bond, an --NR.sup.10 --group or a --CH.sub.2 --NR.sup.10 --group in which R.sup.10 is a hydrogen atom or a C1-4 alkyl group; Y is a methylene group or a carbonyl group; and dotted bonds in a six membered ring represent that said six membered ring has the maximum number of double bonds.

摘要翻译： 公开了氢醌衍生物或其药学上可接受的盐，所述对苯二酚衍生物由式（I）表示：未取代的或被各自独立地选自卤素原子，C 1-4烷基的取代基或取代基取代 和C 1-4烷氧基; R2是氢原子或C1-4烷基; R 3和R 4各自独立地为氢原子或C 1-4烷基; R5是氢原子或C1-4烷基; R6，R7和R8各自独立地为氢原子或C1-4烷基; P是羟基; Q是羟基，C 1-4烷氧基，C 1-18酰氧基或氧代基; P可与Q形成醚键; R是羟基，C 1-4烷氧基，C 1-18酰氧基或氧代基，条件是当所述Q和所述R中的一个是氧代基时，另一个也是氧代基; X是单键，-NR 10 - 基或-CH 2 -NR 10 - 基，其中R 10是氢原子或C 1-4烷基; Y是亚甲基或羰基; 六元环中的点状键表示所述六元环具有最大数量的双键。

公开(公告)号：US07754728B2

公开(公告)日：2010-07-13

申请号：US10528343

申请日：2003-09-26

申请人： Yoshiaki Isobe ,  Haruo Takaku ,  Haruhisa Ogita ,  Masanori Tobe ,  Ayumu Kurimoto ,  Tetsuhiro Ogino ,  Hitoshi Fujita

发明人： Yoshiaki Isobe ,  Haruo Takaku ,  Haruhisa Ogita ,  Masanori Tobe ,  Ayumu Kurimoto ,  Tetsuhiro Ogino ,  Hitoshi Fujita

IPC分类号： C07D473/18 ,  C07D473/16 ,  A61K31/522 ,  A61P11/06 ,  A61P37/08

CPC分类号： A61K31/5377 ,  A61K31/522 ,  A61K31/55

摘要： A drug for topically administration which is effective as an antiallergic agent. The drug for topically administration contains as an active ingredient an adenine compound represented by the general formula (1): [wherein ring A represents a 6 to 10 membered, mono or bicyclic, aromatic hydrocarbon or a 5 to 10 membered, mono or bicyclic, aromatic heterocycle containing one to three heteroatoms selected among 0 to 2 nitrogen atoms, 0 or 1 oxygen atom, and 0 or 1 sulfur atom; n is an integer of 0 to 2; m is an integer of 0 to 2; R represents halogeno, (un)substituted alkyl, etc.; X1 represents oxygen, sulfur, NR1 (R1 represents hydrogen or alkyl), or a single bond; Y1 represents a single bond, alkylene, etc.; Y2 represents a single bond, alkylene, etc.; Z represents alkylene; and at least one of Q1 and Q2 represents —COOR10 (wherein R10 represents (un)substituted alkyl, etc.), etc.] or a pharmaceutically acceptable salt of the compound.

摘要翻译： 用作局部给药的药物，其作为抗过敏剂有效。 用于局部给药的药物含有作为活性成分的由通式（1）表示的腺嘌呤化合物：[其中环A表示6至10元，单或双环，芳族烃或5至10元，单或双环， 含有1至3个选自0至2个氮原子，0或1个氧原子和0或1个硫原子的杂原子的芳族杂环; n为0〜2的整数， m为0〜2的整数; R代表卤代，（取代）烷基等; X1代表氧，硫，NR1（R1代表氢或烷基）或单键; Y1表示单键，亚烷基等; Y2表示单键，亚烷基等; Z表示亚烷基; 并且Q1和Q2中的至少一个表示-COOR 10（其中R 10表示（un）取代的烷基等）等）或该化合物的药学上可接受的盐。

公开(公告)号：US06376501B1

公开(公告)日：2002-04-23

申请号：US09582176

申请日：2000-06-21

申请人： Yoshiaki Isobe ,  Haruhisa Ogita ,  Masanori Tobe ,  Haruo Takaku ,  Hiroyuki Matsui ,  Hideyuki Tomizawa

发明人： Yoshiaki Isobe ,  Haruhisa Ogita ,  Masanori Tobe ,  Haruo Takaku ,  Hiroyuki Matsui ,  Hideyuki Tomizawa

IPC分类号： A61K3152

CPC分类号： A61K31/522 ,  A61K31/52 ,  C07D473/00 ,  C07D473/34

摘要： The present invention relates to a type 2 helper T cell-selective immune response inhibitor, an immune response regulator and an anti-allergic agent, individually comprising, as an active ingredient, a purine derivative represented by General Formula (I): wherein R2 is hydrogen or a hydrocarbon group in which —CH2— not directly bound to the purine skeleton may be substituted by CO, SO2, O or S, and C—H not directly bound to the purine skeleton may be substituted by N, C-halogen or C—CN; R6 is hydroxyl, amino or amino which is mono- or di-substituted by a hydrocarbon group(s); R8 is hydroxyl, mercapto, acyloxy or hydrocarbon group-substituting oxycarbonyloxy; and R9 is a hydrocarbon group in which —CH2— not directly bound to the purine skeleton may be substituted by CO, SO2, O or S, and C—H not directly bound to the purine skeleton may be substituted by N, C-halogen or C—CN; or its tautomer or a salt of the purine derivative or the tautomer.

摘要翻译： 本发明涉及一种2型辅助性T细胞选择性免疫应答抑制剂，免疫应答调节剂和抗过敏剂，其各自包含作为活性成分的由通式（I）表示的嘌呤衍生物：其中R 2为氢 或其中不直接结合嘌呤骨架的-CH 2可以被CO，SO 2，O或S取代的烃基，并且不直接键合到嘌呤骨架上的CH可以被N，C-卤素或C-CN R6是羟基，被一个或多个烃基单取代或二取代的氨基或氨基; R8是羟基，巯基，酰氧基或烃基取代的氧羰基氧基; 并且R 9是其中不直接结合嘌呤骨架的-CH 2可以被CO，SO 2，O或S取代的烃基，并且不直接键合到嘌呤骨架上的CH可以被N，C-卤素或C- CN;或其互变异构体或嘌呤衍生物或互变异构体的盐。

公开(公告)号：US20120178743A1

公开(公告)日：2012-07-12

申请号：US13402850

申请日：2012-02-22

申请人： Yoshiaki ISOBE ,  Haruo Takaku ,  Haruhisa Ogita ,  Masanori Tobe ,  Ayumu Kurimoto ,  Tetsuhiro Ogino ,  Hitoshi Fujita

发明人： Yoshiaki ISOBE ,  Haruo Takaku ,  Haruhisa Ogita ,  Masanori Tobe ,  Ayumu Kurimoto ,  Tetsuhiro Ogino ,  Hitoshi Fujita

IPC分类号： A61K31/52 ,  A61K31/5377 ,  A61P37/08 ,  A61P37/00 ,  A61P31/12 ,  A61P17/00 ,  C07D473/18 ,  A61K31/55

CPC分类号： A61K31/5377 ,  A61K31/522 ,  A61K31/55

摘要： An antiallergic agent for topical administration containing an adenine compound of general formula (1): [wherein ring A represents a 6 to 10 membered, mono or bicyclic, aromatic hydrocarbon or a 5 to 10 membered, mono or bicyclic, aromatic heterocycle containing one to three heteroatoms selected among 0 to 2 nitrogen atoms, 0 or 1 oxygen atom, and 0 or 1 sulfur atom; n is an integer of 0 to 2; m is an integer of 0 to 2; R represents halogeno, (un)substituted alkyl, etc.; X1 represents oxygen, sulfur, NR1 (R1 represents hydrogen or alkyl), or a single bond; Y1 represents a single bond, alkylene, etc.; Y2 represents a single bond, alkylene, etc.; Z represents alkylene; and at least one of Q1 and Q2 represents —COOR10 (wherein R10 represents (un)substituted alkyl, etc.), etc.] or a pharmaceutically acceptable salt of the compound.

摘要翻译： 一种用于局部给药的抗过敏剂，其含有通式（1）的腺嘌呤化合物：[其中环A表示6至10元，单或双环，芳烃或5至10元单或双环芳族杂环， 选自0至2个氮原子，0或1个氧原子和0或1个硫原子的3个杂原子; n为0〜2的整数， m为0〜2的整数; R代表卤代，（取代）烷基等; X1代表氧，硫，NR1（R1代表氢或烷基）或单键; Y1表示单键，亚烷基等; Y2表示单键，亚烷基等; Z表示亚烷基; 并且Q1和Q2中的至少一个表示-COOR 10（其中R 10表示（un）取代的烷基等）等）或该化合物的药学上可接受的盐。

公开(公告)号：US07157465B2

公开(公告)日：2007-01-02

申请号：US10474199

申请日：2002-04-15

申请人： Yoshiaki Isobe ,  Haruhisa Ogita ,  Masanori Tobe ,  Haruo Takaku ,  Tetsuhiro Ogino ,  Ayumu Kurimoto ,  Hajime Kawakami

发明人： Yoshiaki Isobe ,  Haruhisa Ogita ,  Masanori Tobe ,  Haruo Takaku ,  Tetsuhiro Ogino ,  Ayumu Kurimoto ,  Hajime Kawakami

IPC分类号： C07D473/16 ,  C07D473/18 ,  C07D473/24 ,  A61K31/52 ,  A61K31/522

CPC分类号： C07D473/00 ,  C07D473/16 ,  C07D473/18 ,  C07D473/24 ,  C07D473/34

摘要： This invention relates to an adenine derivative, a tautomer thereof, or a pharmaceutically acceptable salt thereof represented by general formula (I): wherein X represents NR3 (wherein R3 represents a hydrogen atom or C1-3 alkyl) or the like; R1 represents substituted or unsubstituted alkyl or the like; R2 represents hydroxyl or the like; and Y represents a substituted or unsubstituted aromatic hetero ring or the like. Also, the present invention relates to pharmaceuticals such as an interferon inducer, antiviral agent, anticancer agent, type 2 helper T cell selective immune response inhibitor, antiallergic agent, and immune response modulator comprising the above derivative as an active ingredient.

摘要翻译： 本发明涉及由通式（I）表示的腺嘌呤衍生物，其互变异构体或其药学上可接受的盐：其中X表示NR 3（其中R 3表示 氢原子或C 1-3烷基）等; R 1表示取代或未取代的烷基等; R 2表示羟基等; Y表示取代或未取代的芳族杂环等。 此外，本发明涉及包含上述衍生物作为活性成分的药物，例如干扰素诱导剂，抗病毒剂，抗癌剂，2型辅助T细胞选择性免疫应答抑制剂，抗过敏剂和免疫应答调节剂。

公开(公告)号：US20100256118A1

公开(公告)日：2010-10-07

申请号：US12793649

申请日：2010-06-03

申请人： Yoshiaki ISOBE ,  Haruo Takaku ,  Haruhisa Ogita ,  Masanori Tobe ,  Ayumu Kurimoto ,  Tetsuhiro Ogino ,  Hitoshi Fujita

发明人： Yoshiaki ISOBE ,  Haruo Takaku ,  Haruhisa Ogita ,  Masanori Tobe ,  Ayumu Kurimoto ,  Tetsuhiro Ogino ,  Hitoshi Fujita

IPC分类号： A61K31/52 ,  C07D473/18 ,  A61K31/5377 ,  C07D473/24 ,  C07D473/16 ,  A61K31/55 ,  A61P11/06 ,  A61P17/00 ,  A61P37/02

CPC分类号： A61K31/5377 ,  A61K31/522 ,  A61K31/55

摘要： A drug for topically administration which is effective as an antiallergic agent. The drug for topically administration contains as an active ingredient an adenine compound represented by the general formula (1): [wherein ring A represents a 6 to 10 membered, mono or bicyclic, aromatic hydrocarbon or a 5 to 10 membered, mono or bicyclic, aromatic heterocycle containing one to three heteroatoms selected among 0 to 2 nitrogen atoms, 0 or 1 oxygen atom, and 0 or 1 sulfur atom; n is an integer of 0 to 2; m is an integer of 0 to 2; R represents halogeno, (un)substituted alkyl, etc.; X1 represents oxygen, sulfur, NR1 (R1 represents hydrogen or alkyl), or a single bond; Y1 represents a single bond, alkylene, etc.; Y2 represents a single bond, alkylene, etc.; Z represents alkylene; and at least one of Q1 and Q2 represents —COOR10 (wherein R10 represents (un)substituted alkyl, etc.), etc.] or a pharmaceutically acceptable salt of the compound.

摘要翻译： 用作局部给药的药物，其作为抗过敏剂有效。 用于局部给药的药物含有作为活性成分的由通式（1）表示的腺嘌呤化合物：[其中环A表示6至10元，单或双环，芳族烃或5至10元，单或双环， 含有1至3个选自0至2个氮原子，0或1个氧原子和0或1个硫原子的杂原子的芳族杂环; n为0〜2的整数， m为0〜2的整数; R代表卤代，（取代）烷基等; X1代表氧，硫，NR1（R1代表氢或烷基）或单键; Y1表示单键，亚烷基等; Y2表示单键，亚烷基等; Z表示亚烷基; 并且Q1和Q2中的至少一个表示-COOR 10（其中R 10表示（un）取代的烷基等）等）或该化合物的药学上可接受的盐。

公开(公告)号：US07521454B2

公开(公告)日：2009-04-21

申请号：US11582452

申请日：2006-10-18

申请人： Yoshiaki Isobe ,  Haruhisa Ogita ,  Masanori Tobe ,  Haruo Takaku ,  Tetsuhiro Ogino ,  Ayumu Kurimoto ,  Hajime Kawakami

发明人： Yoshiaki Isobe ,  Haruhisa Ogita ,  Masanori Tobe ,  Haruo Takaku ,  Tetsuhiro Ogino ,  Ayumu Kurimoto ,  Hajime Kawakami

IPC分类号： A61P11/06 ,  A61P17/00 ,  A61P35/00 ,  C07D473/16 ,  C07D473/18 ,  C07D473/24 ,  A61K31/52 ,  A61K31/522

CPC分类号： C07D473/00 ,  C07D473/16 ,  C07D473/18 ,  C07D473/24 ,  C07D473/34

摘要： This invention relates to an adenine derivative, a tautomer thereof, or a pharmaceutically acceptable salt thereof represented by general formula (I): wherein X represents NR3 (wherein R3 represents a hydrogen atom or C1-3 alkyl) or the like; R1 represents substituted or unsubstituted alkyl or the like; R2 represents hydroxyl or the like; and Y represents a substituted or unsubstituted aromatic hetero ring or the like. Also, the present invention relates to pharmaceuticals such as an interferon inducer, antiviral agent, anticancer agent, type 2 helper T cell selective immune response inhibitor, antiallergic agent, and immune response modulator comprising the above derivative as an active ingredient.

摘要翻译： 本发明涉及由通式（I）表示的腺嘌呤衍生物，其互变异构体或其药学上可接受的盐：其中X表示NR 3（其中R 3表示氢原子或C 1-3烷基）等; R 1表示取代或未取代的烷基等; R2表示羟基等; Y表示取代或未取代的芳族杂环等。 此外，本发明涉及包含上述衍生物作为活性成分的药物，例如干扰素诱导剂，抗病毒剂，抗癌剂，2型辅助T细胞选择性免疫应答抑制剂，抗过敏剂和免疫应答调节剂。

公开(公告)号：US20060094737A1

公开(公告)日：2006-05-04

申请号：US10528373

申请日：2003-09-17

申请人： Yoshiaki Isobe ,  Masanori Tobe ,  Yoshifumi Inoue ,  Masakazu Isobe

发明人： Yoshiaki Isobe ,  Masanori Tobe ,  Yoshifumi Inoue ,  Masakazu Isobe

IPC分类号： A61K31/513 ,  C07D405/02 ,  C07D239/54

CPC分类号： C07D239/545 ,  A61K31/513 ,  C07D405/06 ,  C07D405/12 ,  C07D405/14

摘要： It is intended to provide an uracil derivative represented by the following general formula (I): (I) wherein X represents a group selected from among NHCO, NHCH2, CO, CONH and CH2NH; R1 represents hydrogen or optionally substituted C1-6 alkyl; R2 represents a group of the following general formula (II) or (III): (II) (III) (wherein m is 0 or 1; n is an integer of from 1 to 3; Y represents OH or NH2; and a dotted line shows a binding position), provided that when R2 is a group of the general formula (III), X represents NHCO or NHCH2; R3 and R4 independently represent each hydrogen or C1-6 alkyl; and Ar represents phenyl substituted by C1-6 alkyl at the o- and m-positions, optionally substituted heteroaryl or a bicyclic aromatic group; its pharmaceutically acceptable salt, and a remedy containing the above uracil derivative or its pharmaceutically acceptable salt as the active ingredient for, in particular, allergic diseases relating to a type IV allergic reaction, i.e., a novel compound useful in treating diseases in which a type IV allergic reaction participates and a remedy for allergic diseases containing the same as the active ingredient.

摘要翻译： 旨在提供由以下通式（I）表示的尿嘧啶衍生物：（I）其中X表示选自NHCO，NHCH 2，CO，CONH和CH 2的基团 NH; R 1表示氢或任选取代的C 1-6烷基; R 2表示下述通式（II）或（III）的基团：（II）（III）（其中m为0或1; n为1至3的整数; Y 表示OH或NH 2，虚线表示结合位置），条件是当R 2为通式（III）的基团时，X表示NHCO或 NHCH 2

公开(公告)号：US08148371B2

公开(公告)日：2012-04-03

申请号：US12793649

申请日：2010-06-03

申请人： Yoshiaki Isobe ,  Haruo Takaku ,  Haruhisa Ogita ,  Masanori Tobe ,  Ayumu Kurimoto ,  Tetsuhiro Ogino ,  Hitoshi Fujita

发明人： Yoshiaki Isobe ,  Haruo Takaku ,  Haruhisa Ogita ,  Masanori Tobe ,  Ayumu Kurimoto ,  Tetsuhiro Ogino ,  Hitoshi Fujita

IPC分类号： C07D473/18 ,  A61K31/522 ,  A61P37/08 ,  A61P11/06 ,  C07D473/40 ,  C07D473/16

CPC分类号： A61K31/5377 ,  A61K31/522 ,  A61K31/55

摘要： A drug for topically administration which is effective as an antiallergic agent. The drug for topically administration contains as an active ingredient an adenine compound represented by the general formula (1): [wherein ring A represents a 6 to 10 membered, mono or bicyclic, aromatic hydrocarbon or a 5 to 10 membered, mono or bicyclic, aromatic heterocycle containing one to three heteroatoms selected among 0 to 2 nitrogen atoms, 0 or 1 oxygen atom, and 0 or 1 sulfur atom; n is an integer of 0 to 2; m is an integer of 0 to 2; R represents halogeno, (un)substituted alkyl, etc.; X1 represents oxygen, sulfur, NR1 (R1 represents hydrogen or alkyl), or a single bond; Y1 represents a single bond, alkylene, etc.; Y2 represents a single bond, alkylene, etc.; Z represents alkylene; and at least one of Q1 and Q2 represents —COOR10 (wherein R10 represents (un)substituted alkyl, etc.), etc.] or a pharmaceutically acceptable salt of the compound.

摘要翻译： 用作局部给药的药物，其作为抗过敏剂有效。 用于局部给药的药物含有作为活性成分的由通式（1）表示的腺嘌呤化合物：[其中环A表示6至10元，单或双环，芳族烃或5至10元，单或双环， 含有1至3个选自0至2个氮原子，0或1个氧原子和0或1个硫原子的杂原子的芳族杂环; n为0〜2的整数， m为0〜2的整数; R代表卤代，（取代）烷基等; X1代表氧，硫，NR1（R1代表氢或烷基）或单键; Y1表示单键，亚烷基等; Y2表示单键，亚烷基等; Z表示亚烷基; 并且Q1和Q2中的至少一个表示-COOR 10（其中R 10表示（un）取代的烷基等）等）或该化合物的药学上可接受的盐。