公开(公告)号：US20110136801A1

公开(公告)日：2011-06-09

申请号：US12958846

申请日：2010-12-02

申请人： Yoshiaki Isobe ,  Mai Kasai ,  Tomoaki Nakamura ,  Shingo Tojo ,  Hirotaka Kurebayashi

发明人： Yoshiaki Isobe ,  Mai Kasai ,  Tomoaki Nakamura ,  Shingo Tojo ,  Hirotaka Kurebayashi

IPC分类号： A61K31/4745 ,  C07D471/04 ,  A61K31/496 ,  A61K31/5377 ,  A61P35/00 ,  A61P31/04 ,  A61P31/12 ,  A61P11/06 ,  A61P17/00 ,  A61P31/18 ,  A61P31/20 ,  A61P31/14

CPC分类号： C07D471/04

摘要： The present invention provides compounds of formula (I): wherein Ra, Rb, Rc, R1, R2, R3, X1, Y1, Z1, A, n and m are as defined in the specification, and pharmaceutically acceptable salts thereof, as well as processes for their preparation, pharmaceutical compositions containing them and their use in therapy.

摘要翻译： 本发明提供式（I）化合物：其中Ra，Rb，Rc，R 1，R 2，R 3，X 1，Y 1，Z 1，A，n和m如说明书中所定义，及其药学上可接受的盐 作为其制备方法，含有它们的药物组合物及其在治疗中的用途。

公开(公告)号：US20080269240A1

公开(公告)日：2008-10-30

申请号：US12067446

申请日：2006-09-21

申请人： Kazuki Hashimoto ,  Tomoaki Nakamura ,  Kei Nakamura ,  Shingo Tojo ,  Ayumu Kurimoto ,  Yoshiaki Isobe ,  Hiroki Wada ,  Roger Bonnert

发明人： Kazuki Hashimoto ,  Tomoaki Nakamura ,  Kei Nakamura ,  Shingo Tojo ,  Ayumu Kurimoto ,  Yoshiaki Isobe ,  Hiroki Wada ,  Roger Bonnert

IPC分类号： A61K31/522 ,  C07D473/18 ,  A61P31/12

CPC分类号： C07D473/18

摘要： An adenine compound useful as a medicine represented by the following formula (1): [wherein R1 is halogen atom, optionally substituted alkyl group, optionally substituted aryl group, etc.; X is oxygen atom, sulfur atom, a single bond, etc.; A1 is optionally substituted and optionally saturated 4 to 8 membered heterocyclic group containing 1 to 2 hetero atoms selected from 1 to 3 nitrogen atoms, 0 to 1 oxygen atom, and 0 to 1 sulfur atom; A2 is optionally substituted 6 to 10 cyclic aromatic hydrocarbon group or optionally substituted 5 to 10 membered heterocyclic aromatic group; L1 and L2 are independently, substituted straight or branched alkylene or a single bond, etc.; L3 is optionally substituted straight or branched alkylene, etc.; R2 is hydrogen atom, optionally substituted alkyl group.] or its pharmaceutically acceptable salt.

摘要翻译： 用作下式（1）表示的药物的腺嘌呤化合物：其中R 1是卤素原子，任选取代的烷基，任选取代的芳基等; X是氧原子，硫原子，单键等; 任选被取代的和任选饱和的含有1至2个选自1至3个氮原子，0至1个氧原子和0至1个硫原子的杂原子的4至8元杂环基; 任选取代的6至10个环状芳族烃基或任选取代的5至10元杂环芳基; L 1和L 2独立地为取代的直链或支链亚烷基或单键等; L 3是任选取代的直链或支链亚烷基等; R 2是氢原子，任选取代的烷基。]或其药学上可接受的盐。

公开(公告)号：US20090082332A1

公开(公告)日：2009-03-26

申请号：US12067536

申请日：2006-09-20

申请人： Philip Abbot ,  Roger Victor Bonnert ,  Stephen Brough ,  Kamaldeep Chohan ,  Thomas McInally ,  Stephen Thom ,  Yoshiaki Isobe ,  Kei Nakamura ,  Shingo Tojo

发明人： Philip Abbot ,  Roger Victor Bonnert ,  Stephen Brough ,  Kamaldeep Chohan ,  Thomas McInally ,  Stephen Thom ,  Yoshiaki Isobe ,  Kei Nakamura ,  Shingo Tojo

IPC分类号： A61K31/397 ,  C07D473/02 ,  A61P31/12 ,  A61P35/00 ,  A61P37/08 ,  A61K31/522

CPC分类号： C07D473/34

摘要： The present invention provides compounds of formula (I) wherein R1, Y1, X1, Z1, X2, Y2, A, Y3, n, R and R2 are as defined in the specification, processes for their preparation, pharmaceutical compositions containing them and their use in therapy.

摘要翻译： 本发明提供式（I）化合物，其中R1，Y1，X1，Z1，X2，Y2，A，Y3，n，R和R2如说明书中所定义，其制备方法，含有它们的药物组合物及其制备方法 用于治疗。

公开(公告)号：US20100099870A1

公开(公告)日：2010-04-22

申请号：US12531867

申请日：2008-03-19

申请人： Yoshiaki Isobe ,  Tomoaki Nakamura

发明人： Yoshiaki Isobe ,  Tomoaki Nakamura

IPC分类号： C07D473/18

CPC分类号： C07D473/18 ,  C07D473/00

摘要： A novel adenine compound represented by the formula (1): [wherein R1 is substituted or unsubstituted alkyl, etc., X is oxygen, etc., A1 is 4- to 8-membered substituted or unsubstituted saturated nitrogen-containing heterocycle containing 1 to 2 hetero atom(s) selected from 1 to 2 nitrogen(s), 0 to 1 oxygen and 0 to 1 sulfur, etc., A2 is substituted or unsubstituted 6- to 10-membered aryl, etc., L1 and L2 are independently a straight chain or branched chain alkylene, etc.], or a pharmaceutically acceptable salt thereof, which is useful as a medicament.

摘要翻译： 由式（1）表示的新型腺嘌呤化合物：其中，R 1为取代或未取代的烷基等，X为氧等，A 1为4〜8元的取代或未取代的饱和含氮杂环， 2个选自1至2个氮，0至1个氧和0至1个硫等的杂原子，A2为取代或未取代的6-至10-元芳基等，L1和L2独立地为 直链或支链亚烷基等]或其药学上可接受的盐，其可用作药物。

公开(公告)号：US20100093998A1

公开(公告)日：2010-04-15

申请号：US12532007

申请日：2008-03-19

申请人： Yoshiaki Isobe ,  Tomoaki Nakamura

发明人： Yoshiaki Isobe ,  Tomoaki Nakamura

IPC分类号： C07D473/18

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

摘要： A novel adenine compound represented by the formula (1): wherein A represents an (un)substituted aromatic carbocycle or (un)substituted aromatic heterocycle; L1 and L2 each independently represents straighted or branched alkylene, etc.; R1 represents halogen, (un)substituted alkyl, (un)substituted alkenyl, (un)substituted alkynyl, (un)substituted cycloalkyl, (un)substituted aryl, or (un)substituted heteroaryl; R2 and R3 each independently represents hydrogen, or (un)substituted alkyl, (un)substituted alkenyl, (un)substituted alkynyl, (un)substituted cycloalkyl, (un)substituted saturated heterocycle, (un)substituted aryl, or (un)substituted heteroaryl, or R2 combines together with L2 or R3 to form (un)substituted 4- to 8-membered nitrogen-containing saturated heterocycle; X is oxygen, sulfur, SO, SO2, NR7, NR7CO wherein R7 is hydrogen or alkyl, or a single bond; provided that X is a single bond when R1 is halogen, or a pharmaceutically acceptable salt thereof. The compound and salt are useful as a medicine.

摘要翻译： 由式（1）表示的新型腺嘌呤化合物：其中A表示（un）取代的芳族碳环或（un）取代的芳族杂环; L1和L2各自独立地表示直链或支链亚烷基等; R 1表示卤素，（未）取代的烷基，（未）取代的烯基，（未）取代的炔基，（未）取代的环烷基，（未）取代的芳基或（未）取代的杂芳基; R2和R3各自独立地表示氢，或（未）取代的烷基，（未）取代的烯基，（未）取代的炔基，（未）取代的环烷基，（未）取代的饱和杂环，（未）取代的芳基或（未） 或R 2与L 2或R 3一起形成（未）取代的4-至8-元含氮饱和杂环; X是氧，硫，SO，SO 2，NR 7，NR 7 CO，其中R 7是氢或烷基，或单键; 条件是当R 1为卤素时X为单键，或其药学上可接受的盐。 化合物和盐可用作药物。

公开(公告)号：US20090118263A1

公开(公告)日：2009-05-07

申请号：US12067649

申请日：2006-09-20

申请人： Kazuki Hashimoto ,  Tomoaki Nakamura ,  Kei Nakamura ,  Ayumu Kurimoto ,  Yoshiaki Isobe

发明人： Kazuki Hashimoto ,  Tomoaki Nakamura ,  Kei Nakamura ,  Ayumu Kurimoto ,  Yoshiaki Isobe

IPC分类号： A61K31/551 ,  C07D473/00 ,  A61K31/522 ,  C07D413/02 ,  A61K31/5386 ,  A61P37/08 ,  A61P35/00 ,  A61P37/02 ,  A61K31/5377 ,  A61K31/496 ,  C07D243/08

CPC分类号： C07D473/16 ,  C07D473/18 ,  C07D519/00

摘要： An adenine compound represented by the formula (1): (1) [wherein A1 and A2 each independently represents an (un)substituted aromatic carbocycle or (un)substituted aromatic heterocycle; L1, L2, and L3 each independently represents alkylene or a single bond, provided that any methylene or methine group in L2 or L3 may be bonded to the nitrogen atom adjacent to L2 and L3 to form a 4- to 7-membered saturated nitrogenous heterocycle; L4 represents alkylene or a single bond; R1 represents (un)substituted alkyl, (un)substituted aryl, etc.; R2 represents hydrogen or (un)substituted alkyl; R3 represents (un)substituted alkyl, etc.; and X represents oxygen, etc.] or a pharmaceutically acceptable salt of the compound. The compound and salt are useful as a medicine.

摘要翻译： 由式（1）表示的腺嘌呤化合物：（1）[其中，A1和A2各自独立地表示（un）取代的芳族碳环或（un）取代的芳族杂环; L1，L2和L3各自独立地表示亚烷基或单键，条件是L2或L3中的任何亚甲基或次甲基可以键合到与L2和L3相邻的氮原子上以形成4-至7-元饱和含氮杂环 ; L4表示亚烷基或单键; R1表示（un）取代的烷基，（un）取代的芳基等; R2代表氢或（未）取代的烷基; R3表示（un）取代的烷基等; X表示氧等]或化合物的药学上可接受的盐。 化合物和盐可用作药物。

公开(公告)号：US20090192153A1

公开(公告)日：2009-07-30

申请号：US12067780

申请日：2006-09-21

申请人： Kazuki Hashimoto ,  Tomoaki Nakamura ,  Kei Nakamura ,  Ayumu Kurimoto ,  Yoshiaki Isobe ,  Haruhisa Ogita ,  Ian Millichip ,  Thomas Mcinally ,  Roger Bonnert

发明人： Kazuki Hashimoto ,  Tomoaki Nakamura ,  Kei Nakamura ,  Ayumu Kurimoto ,  Yoshiaki Isobe ,  Haruhisa Ogita ,  Ian Millichip ,  Thomas Mcinally ,  Roger Bonnert

IPC分类号： A61K31/5377 ,  C07D473/34 ,  A61K31/522 ,  A61P37/08

CPC分类号： C07D473/18

摘要： An adenine compound or its pharmaceutically acceptable salt as a medicament as shown following formula (1): wherein R1 is optionally substituted alkyl group, etc., X is oxygen atom, etc., A is 4 to 8 membered optionally substituted saturated or unsaturated heterocyclic group containing 1 to 2 hetero atoms selected from 1 to 3 nitrogen atoms, 0 to 1 oxygen atom and 0 to 1 sulfur atom, L1 and L2 are independently straight or branched chain alkylene, or a single bond, R2 is optionally substituted alkyl group, etc.

摘要翻译： 腺嘌呤化合物或其药学上可接受的盐作为如下式（1）所示的药物：其中R 1是任选取代的烷基等，X是氧原子等，A是4至8元任选取代的饱和或不饱和杂环 含有1至2个选自1至3个氮原子，0至1个氧原子和0至1个硫原子的杂原子的基团，L1和L2独立地为直链或支链亚烷基或单键，R2为任选取代的烷基， 等等

公开(公告)号：US20070225303A1

公开(公告)日：2007-09-27

申请号：US10594074

申请日：2005-03-25

申请人： Haruhisa Ogita ,  Tomoaki Nakamura ,  Yoshiaki Isobe ,  Kazuki Hashimoto ,  Ayumu Kurimoto

发明人： Haruhisa Ogita ,  Tomoaki Nakamura ,  Yoshiaki Isobe ,  Kazuki Hashimoto ,  Ayumu Kurimoto

IPC分类号： A61K31/522 ,  C07D473/34

CPC分类号： C07D473/16 ,  A61K31/522 ,  A61K31/5377 ,  C07D473/18 ,  C07D473/24 ,  C07D473/34

摘要： An 8-oxoadenine compound useful as an immuno-modulator having specific activity against Th1/Th2, specifically a prophylactic and therapeutic agent for a topical application for allergic diseases, viral diseases and cancers, which is represented by the following formula (1): wherein A is a group of a formula represented by the formula (2): wherein R2 is a substituted or unsubstituted alkyl group and so on, R3 is hydrogen atom or an alkyl group, R is a halogen atom and so on, n is 0˜2, X1 is oxygen atom, Z is straight or branched chain alkylene, and R1 is an alkyl group which is optionally substituted by hydroxy group, an alkoxy group, alkoxycarbonyl group and so on, or its pharmaceutically acceptable salt.

摘要翻译： 可用作对Th1 / Th2具有比活性的免疫调节剂的8-氧基腺嘌呤化合物，特别是用于过敏性疾病，病毒性疾病和癌症的局部应用的预防和治疗剂，其由下式（1）表示：其中 A是由式（2）表示的式的基团：其中R 2是取代或未取代的烷基等，R 3是氢原子或 烷基，R为卤素原子等，n为0〜2，X 1为氧原子，Z为直链或支链亚烷基，R 1为 任选被羟基，烷氧基，烷氧基羰基等取代的烷基或其药学上可接受的盐。

公开(公告)号：US20090105212A1

公开(公告)日：2009-04-23

申请号：US12067651

申请日：2006-09-22

申请人： Yoshiaki Isobe ,  Ayumu Kurimoto ,  Kazuki Hashimoto ,  Tomoaki Nakamura ,  Kei Nakamura

发明人： Yoshiaki Isobe ,  Ayumu Kurimoto ,  Kazuki Hashimoto ,  Tomoaki Nakamura ,  Kei Nakamura

IPC分类号： A61K31/522 ,  C07D473/34 ,  A61P31/18

CPC分类号： C07D473/18

摘要： A novel adenine compound represented by the formula (1): wherein A represents an (un)substituted aromatic carbocycle or (un)substituted aromatic heterocycle; L1, L2, and L3 each independently represents linear or branched alkylene, etc.; R1 represents (un)substituted alkyl, (un)substituted aryl, etc.; R2 represents hydrogen or (un) substituted alkyl; R3 represents (un)substituted alkyl, etc., provided that R3 may be bonded to L2 or L3 to form a nitrogenous saturated heterocycle; and X represents oxygen, etc.; or a pharmaceutically acceptable salt of the compound. The compound and salt are useful as a medicine.

摘要翻译： 由式（1）表示的新型腺嘌呤化合物：其中A表示（un）取代的芳族碳环或（un）取代的芳族杂环; L1，L2和L3各自独立地表示直链或支链亚烷基等; R1表示（un）取代的烷基，（un）取代的芳基等; R2代表氢或（未）取代的烷基; R3表示（un）取代的烷基等，条件是R3可以键合到L2或L3以形成含氮饱和杂环; X表示氧等。 或该化合物的药学上可接受的盐。 化合物和盐可用作药物。

公开(公告)号：US08044056B2

公开(公告)日：2011-10-25

申请号：US12531867

申请日：2008-03-19

申请人： Yoshiaki Isobe ,  Tomoaki Nakamura

发明人： Yoshiaki Isobe ,  Tomoaki Nakamura

IPC分类号： C07D473/18 ,  A61K31/522 ,  C07D241/08 ,  C07D241/04 ,  A61P37/08 ,  A61P11/06 ,  A61P37/06

CPC分类号： C07D473/18 ,  C07D473/00

摘要： A novel adenine compound represented by the formula (1): [wherein R1 is substituted or unsubstituted alkyl, etc., X is oxygen, etc., A1 is 4- to 8-membered substituted or unsubstituted saturated nitrogen-containing heterocycle containing 1 to 2 hetero atom(s) selected from 1 to 2 nitrogen(s), 0 to 1 oxygen and 0 to 1 sulfur, etc., A2 is substituted or unsubstituted 6- to 10-membered aryl, etc., L1 and L2 are independently a straight chain or branched chain alkylene, etc.], or a pharmaceutically acceptable salt thereof, which is useful as a medicament.

摘要翻译： 由式（1）表示的新型腺嘌呤化合物：其中，R 1为取代或未取代的烷基等，X为氧等，A 1为4〜8元的取代或未取代的饱和含氮杂环， 2个选自1至2个氮，0至1个氧和0至1个硫等的杂原子，A2为取代或未取代的6-至10-元芳基等，L1和L2独立地为 直链或支链亚烷基等]或其药学上可接受的盐，其可用作药物。