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公开(公告)号：US07396842B2
公开(公告)日：2008-07-08
申请号：US11111845
申请日：2005-04-22
IPC分类号： A61K31/44 , C07D417/00
CPC分类号： C07D231/12 , C07D233/56 , C07D249/08 , C07D277/42 , C07D417/04 , C07D417/06 , C07D417/12 , C07D417/14
摘要： A 5-membered cyclic compound of the formula: wherein X is oxygen or sulfur, R1 is hydrogen, substituted or unsubstituted alkyl, etc., R2 is hydrogen, substituted or unsubstituted alkyl, substituted or unsubstituted aryl, etc., Y1 is a direct bond, substituted or unsubstituted alkylene, —CO(CH2)n—, etc., the wavy line means (E)-configuration or (Z)-configuration, R3 is substituted or unsubstituted aryl, etc., Y2 is substituted or unsubstituted alkylene, etc., R4 is hydrogen, substituted or unsubstituted alkanoyl, substituted or unsubstituted alkyl, etc., R5 is hydrogen, etc., or a salt thereof, these compound being able to inhibit infiltration of leukocytes such as eosinophils and lymphocytes, by which being useful for the treatment of various kinds of inflammation.
摘要翻译： 下式的5元环状化合物：其中X是氧或硫，R 1是氢，取代或未取代的烷基等，R 2是氢，被取代的 或未取代的烷基，取代或未取代的芳基等，Y 1是直接键，取代或未取代的亚烷基，-CO（CH 2）n， （E）构型或（Z）构型，R 3是取代或未取代的芳基等。Y 2 - 是取代或未取代的亚烷基等，R 4是氢，取代或未取代的烷酰基，取代或未取代的烷基等，R 5是氢等，或 其盐，这些化合物能够抑制白细胞如嗜酸性粒细胞和淋巴细胞的浸润，由此可用于治疗各种炎症。
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公开(公告)号：US20050222226A1
公开(公告)日：2005-10-06
申请号：US11111845
申请日：2005-04-22
IPC分类号： A61P29/00 , A61P37/06 , A61P37/08 , C07D277/42 , C07D277/56 , C07D417/04 , C07D417/12 , C07D417/14 , C07D521/00 , A61K31/426 , C07D277/38
CPC分类号： C07D231/12 , C07D233/56 , C07D249/08 , C07D277/42 , C07D417/04 , C07D417/06 , C07D417/12 , C07D417/14
摘要： A 5-membered cyclic compound of the formula: wherein X is oxygen or sulfur, R1 is hydrogen, substituted or unsubstituted alkyl, etc., R2 is hydrogen, substituted or unsubstituted alkyl, substituted or unsubstituted aryl, etc., Y1 is a direct bond, substituted or unsubstituted alkylene, —CO(CH2)n—, etc., the wavy line means (E)-configuration or (Z)-configuration, R3 is substituted or unsubstituted aryl, etc., Y2 is substituted or unsubstituted alkylene, etc., R4 is hydrogen, substituted or unsubstituted alkanoyl, substituted or unsubstituted alkyl, etc., R5 is hydrogen, etc., or a salt thereof, these compound being able to inhibit infiltration of leukocytes such as eosinophils and lymphocytes, by which being useful for the treatment of various kinds of inflammation.
摘要翻译： 下式的5元环状化合物：其中X是氧或硫，R 1是氢，取代或未取代的烷基等，R 2是氢，被取代的 或未取代的烷基，取代或未取代的芳基等，Y 1是直接键，取代或未取代的亚烷基，-CO（CH 2）n， （E）构型或（Z）构型，R 3是取代或未取代的芳基等。Y 2 - 是取代或未取代的亚烷基等，R 4是氢，取代或未取代的烷酰基，取代或未取代的烷基等，R 5是氢等，或 其盐，这些化合物能够抑制白细胞如嗜酸性粒细胞和淋巴细胞的浸润，由此可用于治疗各种炎症。
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公开(公告)号：US06919361B2
公开(公告)日：2005-07-19
申请号：US10312692
申请日：2001-06-28
IPC分类号： A61P29/00 , A61P37/06 , A61P37/08 , C07D277/42 , C07D277/56 , C07D417/04 , C07D417/12 , C07D417/14 , C07D521/00 , A61K31/425 , C07P277/08
CPC分类号： C07D231/12 , C07D233/56 , C07D249/08 , C07D277/42 , C07D417/04 , C07D417/06 , C07D417/12 , C07D417/14
摘要： A 5-membered cyclic compound of the formula: wherein X is oxygen or sulfur, R1 is hydrogen, substituted or unsubstituted alkyl, etc., R2 is hydrogen, substituted or unsubstituted alkyl, substituted or unsubstituted aryl, etc., Y1 is a direct bond, substituted or unsubstituted alkylene, —CO(CH2)n—, etc., the wavy line means (E)-configuration or (Z)-configuration, R3 is substituted or unsubstituted aryl, etc., Y2 is substituted or unsubstituted alkylene, etc., R4 is hydrogen, substituted or unsubstituted alkanoyl, substituted or unsubstituted alkyl, etc., R5 is hydrogen, etc., or a salt thereof, these compound being able to inhibit infiltration of leukocytes such as eosinophils and lymphocytes, by which being useful for the treatment of various kinds of inflammation.
摘要翻译： 下式的5元环状化合物：其中X是氧或硫，R 1是氢，取代或未取代的烷基等，R 2是氢，被取代的 或未取代的烷基，取代或未取代的芳基等，Y 1是直接键，取代或未取代的亚烷基，-CO（CH 2）n， （E）构型或（Z）构型，R 3是取代或未取代的芳基等。Y 2 - 是取代或未取代的亚烷基等，R 4是氢，取代或未取代的烷酰基，取代或未取代的烷基等，R 5是氢等，或 其盐，这些化合物能够抑制白细胞如嗜酸性粒细胞和淋巴细胞的浸润，由此可用于治疗各种炎症。
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公开(公告)号：US06458798B1
公开(公告)日：2002-10-01
申请号：US09763728
申请日：2001-02-27
申请人： Hitoshi Fujita , Fujio Antoku , Norio Fujiwara , Kiyotaka Iwai , Hiroshi Tanaka , Hajime Kawakami
发明人： Hitoshi Fujita , Fujio Antoku , Norio Fujiwara , Kiyotaka Iwai , Hiroshi Tanaka , Hajime Kawakami
IPC分类号： C07D23995
CPC分类号： C07D405/04 , C07D405/12 , C07D405/14
摘要： A pyrimidine derivative of the formula (1) or a salt thereof; has an inhibitory activity of production of Th2 type cytokines such as IL-4, IL-5, etc., and is useful as an therapeutic agent for allergic diseases, autoimmune diseases such as systemic lupus erythemathosus, etc., and acquired immunodeficiecy syndrome (AIDS) and so on.
摘要翻译： 式（1）的嘧啶衍生物或其盐具有产生Th2型细胞因子如IL-4，IL-5等的抑制活性，可用作过敏性疾病，自身免疫性疾病的治疗剂 如系统性红斑狼疮等，以及获得性免疫缺陷综合征（AIDS）等。
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公开(公告)号：US06951866B2
公开(公告)日：2005-10-04
申请号：US10222922
申请日：2002-08-19
申请人： Hitoshi Fujita , Fujio Antoku , Norio Fujiwara , Kiyotaka Iwai , Hiroshi Tanaka , Hajime Kawakami
发明人： Hitoshi Fujita , Fujio Antoku , Norio Fujiwara , Kiyotaka Iwai , Hiroshi Tanaka , Hajime Kawakami
IPC分类号： C07D405/04 , C07D405/12 , C07D405/14 , C07D491/044 , C07D491/052 , C07D239/49 , A61K31/505 , C07D239/48
CPC分类号： C07D405/04 , C07D405/12 , C07D405/14
摘要： 1. A pyrimidine derivative of the formula (1) or a salt thereof; has an inhibitory activity of production of Th2 type cytokines such as IL-4, IL-5, etc., and is useful as an therapeutic agent for allergic diseases, autoimmune diseases such as systemic lupus erythemathosus, etc., and acquired immunodeficiecy syndrome (AIDS) and so on.
摘要翻译： 1.式（1）的嘧啶衍生物或其盐; 具有产生Th2型细胞因子如IL-4，IL-5等的抑制活性，可用作过敏性疾病，系统性红斑狼疮等自身免疫性疾病等治疗剂，以及获得性免疫缺陷综合征 艾滋病）等。
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公开(公告)号：US4948799A
公开(公告)日：1990-08-14
申请号：US293440
申请日：1989-01-04
申请人： Fujio Antoku , Mayumi Yoshigi , Ikutaro Saji , Atsuyuki Kojima , Kukuo Ishizumi
发明人： Fujio Antoku , Mayumi Yoshigi , Ikutaro Saji , Atsuyuki Kojima , Kukuo Ishizumi
IPC分类号： A61K31/4427 , A61K31/445 , A61K31/4465 , A61K31/451 , A61P25/18 , C07D211/88 , C07D401/06 , C07D417/06 , C07D417/14 , C07D491/18
CPC分类号： C07D401/06 , C07D211/88 , C07D417/06 , C07D417/14
摘要： An imide derivative of the formula: ##STR1## or a pharmaceutically acceptable salt, which is useful as an antipsychotic drug.
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公开(公告)号：US4843078A
公开(公告)日：1989-06-27
申请号：US182085
申请日：1988-04-15
申请人： Kikuo Ishizumi , Fujio Antoku , Isamu Maruyama , Atsuyuki Kojima
发明人： Kikuo Ishizumi , Fujio Antoku , Isamu Maruyama , Atsuyuki Kojima
IPC分类号： C07D213/74 , A61K31/495 , A61K31/505 , A61P25/18 , A61P25/20 , C07D209/76 , C07D213/84 , C07D213/85 , C07D239/42 , C07D401/12 , C07D403/12
CPC分类号： C07D401/12 , C07D209/76 , C07D403/12
摘要： A succinimide derivative of the formula: ##STR1## wherein R is a pyridyl or pyrimidinyl group substituted with at least one member selected from the group consisting of halogen, lower alkyl, lower alkoxy, cyano, benzyloxy, hydroxyl and amino, and n is an integer of 1 or 2, or a pharmaceutically acceptable acid addition salt thereof. The succinimide derivatives are useful as an anti-anxiety drugs.
摘要翻译： 下式的琥珀酰亚胺衍生物，其中R是被选自卤素，低级烷基，低级烷氧基，氰基，苄氧基，羟基和氨基中的至少一个取代的吡啶基或嘧啶基，n是 1或2的整数，或其药学上可接受的酸加成盐。 琥珀酰亚胺衍生物可用作抗焦虑药。
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公开(公告)号：US4812461A
公开(公告)日：1989-03-14
申请号：US100824
申请日：1987-09-25
申请人： Fujio Antoku , Mayumi Yoshigi , Ikutaro Saji , Atsuyuki Kojima , Kukuo Ishizumi
发明人： Fujio Antoku , Mayumi Yoshigi , Ikutaro Saji , Atsuyuki Kojima , Kukuo Ishizumi
IPC分类号： A61K31/4427 , A61K31/445 , A61K31/4465 , A61K31/451 , A61P25/18 , C07D211/88 , C07D401/06 , C07D417/06 , C07D417/14 , C07D491/18
CPC分类号： C07D401/06 , C07D211/88 , C07D417/06 , C07D417/14
摘要： An imide derivative of the formula: ##STR1## or a pharmaceutically acceptable salt, which is useful as an antipsychotic drug.
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公开(公告)号：US4543355A
公开(公告)日：1985-09-24
申请号：US689776
申请日：1985-01-08
申请人： Kikuo Ishizumi , Fujio Antoku , Yukio Asami
发明人： Kikuo Ishizumi , Fujio Antoku , Yukio Asami
IPC分类号： A61K31/40 , A61K31/505 , C07D209/76 , C07D401/12 , C07D403/02 , C07D403/06 , C07D403/12 , C07D491/18 , C07D403/04 , C07D403/14
CPC分类号： C07D401/12 , C07D209/76 , C07D403/12
摘要： Succinimide derivatives representable by the following formula: ##STR1## wherein X and Y are combined to form a group of the formula: ##STR2## (wherein A is an oxygen atom, a methylene group or an ethylene group and a full line accompanying a broken line is a single bond or a double bond) and Z is a hydrogen atom or, X and Z are combined to form a group of the formula: ##STR3## (wherein A and a full line are each as defined above) and Y is a hydrogen atom, R is a phenyl group, optionally substituted with halogen, C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy or trifluoromethyl, a 2-pyridyl group or a 2-pyrimidinyl group and n is an integer of 3 or 4, and pharmaceutically acceptable acid addition salts thereof, which are useful as antianxious substances.
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公开(公告)号：US4937249A
公开(公告)日：1990-06-26
申请号：US262575
申请日：1988-10-25
申请人： Fujio Antoku , Mayumi Yoshigi , Ikutaro Saji , Kikuo Ishizumi
发明人： Fujio Antoku , Mayumi Yoshigi , Ikutaro Saji , Kikuo Ishizumi
IPC分类号： C07D413/14 , C07D417/14 , C07D491/18
CPC分类号： C07D413/14 , C07D417/14
摘要： A compound of the formula: ##STR1## or its acid addition salt, which is useful as a psychotic drug.
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