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1. 发明授权

US5661153A 1-arylpyrimidine derivatives and pharmaceutical use thereof 失效
标题翻译： 1-芳基嘧啶衍生物及其药物用途
公开(公告)号：US5661153A
公开(公告)日：1997-08-26
申请号：US463277
申请日：1995-06-05
申请人： Yoshiaki Isobe , Toshimasa Katagiri , Junko Umezawa , Yuso Goto , Masashi Sasaki , Nobuo Watanabe , Hideharu Sato , Fumihiro Obara
发明人： Yoshiaki Isobe , Toshimasa Katagiri , Junko Umezawa , Yuso Goto , Masashi Sasaki , Nobuo Watanabe , Hideharu Sato , Fumihiro Obara
IPC分类号： C07D239/54 , C07D239/545 , C07D473/04 , C07D473/06 , A61K31/52
CPC分类号： C07D239/545 , C07D473/04 , C07D473/06
摘要： The present invention relates to 1-arylpyrimidine derivatives represented by general formula (I): ##STR1## wherein R.sub.1 is H, alkyl or aralkyl;Ar is 1-naphthyl, or a substituted or unsubstituted phenyl group;R.sub.4 is a substituted phenyl, a substituted styryl, 1-methylcyclohexyl, 4-methylcyclohexyl, 4-oxo-4H-pyran-2-yl or 2-oxo-2H-pyran-5-yl group;R.sub.5 and R.sub.6 are each independently H or alkyl;R.sub.3 is H, and R.sub.7 and R.sub.8 are combined together to be oxo, or else R.sub.3 and R.sub.7 are combined together to be another direct bond, and R.sub.5 and R.sub.8 are combined together to be a direct bond,or pharmaceutically acceptable salts thereof; and methods for treating allergic diseases with such compounds.
摘要翻译：本发明涉及由通式（I）表示的1-芳基嘧啶衍生物：Ar是1-萘基或取代或未取代的苯基; R4是取代的苯基，取代的苯乙烯基，1-甲基环己基，4-甲基环己基，4-氧代-4H-吡喃-2-基或2-氧代-2H-吡喃-5-基; R5和R6各自独立地为H或烷基; R3为H，R7和R8组合在一起为氧代，或者R3和R7组合在一起成为另一个直接键，R5和R8组合在一起成为直接键，或其药学上可接受的盐; 以及用这些化合物治疗过敏性疾病的方法。

2. 发明授权

US5602140A Purine derivatives and suppressants for inflammatory diseases 失效
标题翻译：嘌呤衍生物和抑制剂用于炎性疾病
公开(公告)号：US5602140A
公开(公告)日：1997-02-11
申请号：US410838
申请日：1995-03-27
申请人： Yoshiaki Isobe , Nobuyoshi Chiba , Yuso Goto , Hideharu Sato
发明人： Yoshiaki Isobe , Nobuyoshi Chiba , Yuso Goto , Hideharu Sato
IPC分类号： C07D233/90 , C07D473/30 , A61K31/52
CPC分类号： C07D473/30
摘要： Purine derivatives shown by general formula [I] or pharmacologically acceptable salts thereof. Suppressants for inflammatory diseases containing an effective ingredient of said purine derivative. ##STR1## (wherein, R represents one group selected from the groups composed of H atom, a straight chain alkyl group having 1-10 carbon atoms, a branched chain alkyl group having 3-10 carbon atoms, an alkyl group having 1-10 carbon atoms substituted with one carboxyl group, 4-carboxybenzyl group and phenethyl group).Above mentioned purine derivatives prevent the tissue damages due to mediators such as active oxygen and TXA.sub.2 in the initial stage of inflammation, and prevent the subsequent aggravation of inflammatory responses due to the adhesion of activated leukocytes to the cells in the lesion, and exhibit efficacy as anti-inflammatory drugs in all stages of inflammatory diseases caused by leukocytes.
摘要翻译：由通式[I]表示的嘌呤衍生物或其药理学上可接受的盐。含有所述嘌呤衍生物的有效成分的炎性疾病抑制剂。（I）（I）（其中，R表示选自由H原子，具有1-10个碳原子的直链烷基，具有3-10个碳原子的支链烷基组成的基团中的一个基团， 1-10个碳原子被一个羧基取代，4-羧基苄基和苯乙基）。上述嘌呤衍生物可防止炎症初期由于诸如活性氧和TXA2等介质而导致的组织损伤，并且防止由于活化的白细胞粘附于病变中的细胞而导致的炎性反应的随后恶化，抗炎药物在白细胞引起的炎症性疾病的各个阶段。

3. 发明授权

US5877318A Hydroquinone derivative and pharmaceutical use thereof 失效
标题翻译：对苯二酚衍生物及其药物用途
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。

4. 发明授权

US5821247A Hydroquinone derivative and pharmaceutical use thereof 失效
标题翻译：对苯二酚衍生物及其药物用途
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。

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