公开(公告)号：US4293713A

公开(公告)日：1981-10-06

申请号：US134556

申请日：1980-03-27

申请人： Hajime Fujimura ,  Yasuzo Hiramatsu ,  Takahiro Yabuuchi ,  Masakatu Hisaki ,  Katsuo Takikawa ,  Takaji Honna ,  Hidekazu Miyake ,  Makoto Kajitani

发明人： Hajime Fujimura ,  Yasuzo Hiramatsu ,  Takahiro Yabuuchi ,  Masakatu Hisaki ,  Katsuo Takikawa ,  Takaji Honna ,  Hidekazu Miyake ,  Makoto Kajitani

IPC分类号： A61K31/17 ,  A61P25/04 ,  A61P29/00 ,  C07C67/00 ,  C07C239/00 ,  C07C275/62 ,  C07C127/24

CPC分类号： C07C275/62 ,  Y10S514/916

摘要： A novel 1,1,3,5-substituted biuret compound of the formula: ##STR1## wherein R.sup.1 and R.sup.2 are respectively the same or different, and each are alkyl groups having 1 to 4 carbon atoms; R.sup.3 is a cyclohexyl group or a phenyl group which may be unsubstituted or may have at least one substituent selected from the group consisting of chlorine, bromine, fluorine, methyl, trifluoromethyl, dimethylamino, methoxy, methylthio, nitro and acetyl. The novel 1,1,3,5-substituted biuret compounds are useful as an analgesic, anti-inflammatory and/or anti-pyretic agent.

摘要翻译： 下式的新型1,1,3,5-取代缩二脲化合物：其中R 1和R 2分别相同或不同，并且各自为具有1至4个碳原子的烷基; R3是可以是未取代的或可以具有至少一个选自氯，溴，氟，甲基，三氟甲基，二甲基氨基，甲氧基，甲硫基，硝基和乙酰基的取代基的环己基或苯基。 新型1,1,3,5-取代的缩二脲化合物可用作止痛剂，抗炎剂和/或抗热解剂。

公开(公告)号：US4371544A

公开(公告)日：1983-02-01

申请号：US257418

申请日：1981-04-24

申请人： Hajime Fujimura ,  Yasuzo Hiramatsu ,  Takahiro Yabuuchi ,  Masakatu Hisaki ,  Katsuo Takikawa ,  Takaji Honna ,  Hidekazu Miyake ,  Makoto Kajitani

发明人： Hajime Fujimura ,  Yasuzo Hiramatsu ,  Takahiro Yabuuchi ,  Masakatu Hisaki ,  Katsuo Takikawa ,  Takaji Honna ,  Hidekazu Miyake ,  Makoto Kajitani

IPC分类号： A61K31/17 ,  C07C275/62 ,  C07D295/215

CPC分类号： C07D295/215 ,  A61K31/17 ,  C07C275/62 ,  Y10S514/887 ,  Y10S514/916

摘要： An analgesic, anti-inflammatory or anti-pyretic composition containing 1,1,3,5-substituted biuret compound of the formula, ##STR1## wherein R.sup.1 is a lower alkyl group or a phenyl group; R.sup.2 is a lower alkyl group, a phenyl group or a substituted phenyl group having chlorine atom(s), methyl group(s) or methoxy group(s) as the substituent(s), further R.sup.1 and R.sup.2 may form a single ring containing one or two hetero atoms including the adjacent nitrogen atom; R.sup.3 is a hydrogen atom, a lower alkyl group or a phenyl group; R.sup.4 is a phenyl group, a substituted phenyl group having halogen atom(s), trifluoromethyl group(s), methyl group(s), methoxy group(s), dimethyl-amino group(s), nitro group(s), hydroxyl group(s), acetyl group(s), or methylthio group(s) as the substituent(s), a benzyl group, a cyclohexyl group or a lower alkyl group, as the active ingredient.

摘要翻译： 含有下式的1,1,3,5-取代缩二脲化合物的镇痛，抗炎或抗热解组合物，其中R1是低级烷基或苯基; R2是低级烷基，苯基或具有氯原子的取代苯基，甲基或甲氧基作为取代基，此外，R 1和R 2可以形成含有 一个或两个杂原子，包括相邻的氮原子; R3是氢原子，低级烷基或苯基; R4是苯基，具有卤素原子的取代苯基，三氟甲基，甲基，甲氧基，二甲基 - 氨基，硝基，羟基 基团，乙酰基或甲硫基作为取代基，苄基，环己基或低级烷基作为活性成分。

公开(公告)号：US4350700A

公开(公告)日：1982-09-21

申请号：US257583

申请日：1981-04-27

申请人： Hajime Fujimura ,  Yasuzo Hiramatsu ,  Takahiro Yabuuchi ,  Masakatu Hisaki ,  Katsuo Takikawa ,  Takaji Honna ,  Hidekazu Miyake ,  Makoto Kajitani

发明人： Hajime Fujimura ,  Yasuzo Hiramatsu ,  Takahiro Yabuuchi ,  Masakatu Hisaki ,  Katsuo Takikawa ,  Takaji Honna ,  Hidekazu Miyake ,  Makoto Kajitani

IPC分类号： A61K31/17 ,  C07C273/18 ,  C07C275/62 ,  C07D213/40 ,  C07D213/75 ,  C07D239/42 ,  C07D277/48 ,  C07D317/66 ,  C07D333/36 ,  A61K31/44

CPC分类号： C07D213/40 ,  A61K31/17 ,  C07C273/1863 ,  C07C273/1872 ,  C07D213/75 ,  C07D239/42 ,  C07D277/48 ,  C07D317/66 ,  C07D333/36 ,  Y10S514/825 ,  Y10S514/916

摘要： An analgesic, anti-inflammatory or anti-pyretic composition containing 1,3,5-substituted biuret compound of the formula, ##STR1## wherein R.sup.1 is a hydrogen atom, a lower alkyl group, a substituted lower alkyl group having chlorine atom(s), cyano group(s), dimethylamino group(s), hydroxy group(s), methoxy group(s) or carboxy group(s) as the substituent(s), a lower alkenyl group, a hydroxy group, a methoxy group, an acetyl group or a phenyl group; R.sup.2 is a hydrogen atom, a lower alkyl group or a phenyl group; R.sup.3 is a phenyl group, a substituted phenyl group having halogen atom(s), trifluoromethyl group(s), methyl group(s), methoxy group(s), methylenedioxy group(s), hydroxy group(s), dimethylamino group(s), carboxy group(s) or carboxymethyl group(s) as the substituent(s), a benzyl group, a pyridyl group, a substituted pyridyl group having methyl group(s) as the substituent(s), a pyridylmethyl group, pyrimidinyl group, a thiazolyl group or a thienyl group, as the active ingredient.

摘要翻译： 含有下式的1,3,5-取代缩二脲化合物的镇痛，抗炎或抗裂解组合物，其中R1是氢原子，低级烷基，具有氯原子的取代的低级烷基（s ），氰基，二甲基氨基，羟基，甲氧基或羧基作为取代基，低级烯基，羟基，甲氧基 ，乙酰基或苯基; R2是氢原子，低级烷基或苯基; R3为苯基，具有卤素原子的取代苯基，三氟甲基，甲基，甲氧基，亚甲二氧基，羟基，二甲基氨基（二甲基氨基） s），作为取代基的羧基或羧甲基，苄基，吡啶基，具有甲基取代基的取代的吡啶基，吡啶基甲基， 嘧啶基，噻唑基或噻吩基作为有效成分。

公开(公告)号：US4278672A

公开(公告)日：1981-07-14

申请号：US134555

申请日：1980-03-27

申请人： Hajime Fujimura ,  Yasuzo Hiramatsu ,  Takahiro Yabuuchi ,  Masakatu Hisaki ,  Katsuo Takikawa ,  Takaji Honna ,  Hidekazu Miyake ,  Makoto Kajitani

发明人： Hajime Fujimura ,  Yasuzo Hiramatsu ,  Takahiro Yabuuchi ,  Masakatu Hisaki ,  Katsuo Takikawa ,  Takaji Honna ,  Hidekazu Miyake ,  Makoto Kajitani

IPC分类号： A61K31/17 ,  C07C275/62 ,  C07D295/215 ,  A61K27/00 ,  A61K31/165 ,  A61K31/40 ,  A61K31/445

CPC分类号： C07D295/215 ,  A61K31/17 ,  C07C275/62 ,  Y10S514/887 ,  Y10S514/916

摘要： An analgesic, anti-inflammatory or anti-pyretic composition containing 1,1,3,5-substituted biuret compound of the formula, ##STR1## wherein R.sup.1 is a lower alkyl group or a phenyl group; R.sup.2 is a lower alkyl group, a phenyl group or a substituted phenyl group having chlorine atom(s), methyl group(s) or methoxy group(s) as the substituent(s), further R.sup.1 and R.sup.2 may form a single ring containing one or two hetero atoms including the adjacent nitrogen atom; R.sup.3 is a hydrogen atom, a lower alkyl group or a phenyl group; R.sup.4 is a phenyl group, a substituted phenyl group having halogen atom(s), trifluoromethyl group(s), methyl group(s), methoxy group(s), dimethylamino group(s), nitro group(s), hydroxyl group(s), acetyl group(s) or methylthio group(s) as the substituent(s), a benzyl group, a cyclohexyl group or a lower alkyl group, as the active ingredient.

摘要翻译： 含有下式的1,1,3,5-取代缩二脲化合物的镇痛，抗炎或抗热解组合物，其中R1是低级烷基或苯基; R2是低级烷基，苯基或具有氯原子的取代苯基，甲基或甲氧基作为取代基，此外，R 1和R 2可以形成含有 一个或两个杂原子，包括相邻的氮原子; R3是氢原子，低级烷基或苯基; R4是苯基，具有卤素原子的取代苯基，三氟甲基，甲基，甲氧基，二甲基氨基，硝基，羟基（ s），乙酰基或甲硫基作为取代基，苄基，环己基或低级烷基作为有效成分。

公开(公告)号：US4287207A

公开(公告)日：1981-09-01

申请号：US134411

申请日：1980-03-27

申请人： Hajime Fujmura ,  Yasuzo Hiramatsu ,  Takahiro Yabuuchi ,  Masakatu Hisaki ,  Katsuo Takikawa ,  Takaji Honna ,  Hidekazu Miyake ,  Makoto Kajitani

发明人： Hajime Fujmura ,  Yasuzo Hiramatsu ,  Takahiro Yabuuchi ,  Masakatu Hisaki ,  Katsuo Takikawa ,  Takaji Honna ,  Hidekazu Miyake ,  Makoto Kajitani

IPC分类号： A61K31/17 ,  C07C273/18 ,  C07C275/62 ,  C07D213/40 ,  C07D213/75 ,  C07D239/42 ,  C07D277/48 ,  C07D317/66 ,  C07D333/36 ,  A61K31/145 ,  A61K31/22 ,  A61K31/275

CPC分类号： C07D213/40 ,  A61K31/17 ,  C07C273/1863 ,  C07C273/1872 ,  C07D213/75 ,  C07D239/42 ,  C07D277/48 ,  C07D317/66 ,  C07D333/36 ,  Y10S514/825 ,  Y10S514/916

摘要： An analgesic, anti-inflammatory or anti-pyretic composition containing 1,3,5-substituted biuret compound of the formula, ##STR1## wherein R.sup.1 is a hydrogen atom, a lower alkyl group, a substituted lower alkyl group having chlorine atom(s), cyano group(s), dimethylamino group(s), hydroxy group(s), methoxy group(s) or carboxy group(s) as the substituent(s), a lower alkenyl group, a hydroxy group, a methoxy group, an acetyl group or a phenyl group; R.sup.2 is a hydrogen atom, a lower alkyl group or a phenyl group; R.sup.3 is a phenyl group, a substituted phenyl group having halogen atom(s), trifluoromethyl group(s), methyl group(s), methoxy group(s), methylenedioxy group(s), hydroxy group(s), dimethylamino group(s), carboxy group(s) or carboxymethyl group(s) as the substituent(s), a benzyl group, a pyridyl group, a substituted pyridyl group having methyl group(s) as the substituent(s), a pyridylmethyl group, pyrimidinyl group, a thiazolyl group or a thienyl group, as the active ingredient.

摘要翻译： 含有下式的1,3,5-取代缩二脲化合物的镇痛，抗炎或抗裂解组合物，其中R1是氢原子，低级烷基，具有氯原子的取代的低级烷基（s ），氰基，二甲基氨基，羟基，甲氧基或羧基作为取代基，低级烯基，羟基，甲氧基 ，乙酰基或苯基; R2是氢原子，低级烷基或苯基; R3为苯基，具有卤素原子的取代苯基，三氟甲基，甲基，甲氧基，亚甲二氧基，羟基，二甲基氨基（二甲基氨基） s），作为取代基的羧基或羧甲基，苄基，吡啶基，具有甲基取代基的取代的吡啶基，吡啶基甲基， 嘧啶基，噻唑基或噻吩基作为有效成分。

公开(公告)号：US4518712A

公开(公告)日：1985-05-21

申请号：US275690

申请日：1981-06-22

申请人： Hajime Fujimura ,  Yasuzo Hiramatsu ,  Tomio Yamazaki ,  Shozo Yamada ,  Takaji Honna

发明人： Hajime Fujimura ,  Yasuzo Hiramatsu ,  Tomio Yamazaki ,  Shozo Yamada ,  Takaji Honna

IPC分类号： C07D295/04 ,  C07D295/06 ,  C07D295/073 ,  A01N43/48

CPC分类号： C07D295/073

摘要： An analgesic composition containing as active ingredient a piperazine derivative represented by the general formula (1) ##STR1## wherein R.sub.1 represents a cyclopropylmethyl group, an isopropyl group or an allyl group and R.sub.2 represents a phenyl group having as substituent a halogen atom or a trifluoromethyl group.

摘要翻译： 含有通式（1）表示的哌嗪衍生物作为活性成分的镇痛药组合物，其中R1表示环丙基甲基，异丙基或烯丙基，R 2表示具有卤素原子取代基的苯基 或三氟甲基。