公开(公告)号：US4863924A

公开(公告)日：1989-09-05

申请号：US939025

申请日：1986-12-08

申请人： Takahiro Haga ,  Nobutoshi Yamada ,  Hideo Sugi ,  Toru Koyanagi ,  Hiroshi Okada

发明人： Takahiro Haga ,  Nobutoshi Yamada ,  Hideo Sugi ,  Toru Koyanagi ,  Hiroshi Okada

IPC分类号： C07D213/64 ,  A61K31/44 ,  A61K31/4402 ,  A61K31/4418 ,  A61K31/50 ,  A61K31/505 ,  A61P35/00 ,  C07D213/643 ,  C07D237/14 ,  C07D239/34

CPC分类号： C07D213/643 ,  C07D237/14 ,  C07D239/34

摘要： An N-benzoyl urea compound having the formula: ##STR1## wherein X is a hydrogen atom, a halogen atom or a nitro group, n is an integer of from 1 to 3, and Q is ##STR2## wherein Y.sub.1 is an unsubstituted or substituted alkyl group, or an alkoxy or alkoxycarbonyl group with its alkyl moiety unsubstituted or substituted, Y.sub.2 is a hydrogen atom, a halogen atom, a nitro group, an unsubstituted or substituted alkyl group, or an alkoxy or alkoxycarbonyl group with its alkyl moiety unsubstituted or substituted, Z is a hydrogen atom, a halogen atom, a trifluoromethyl group or a nitro group, and each of A and B is .dbd.CH-- or a nitrogen atom, provided that one of A and B is .dbd.CH-- and the other is a nitrogen atom, with the provisos (1) that when Q is ##STR3## where when X is a hydrogen atom and Y.sub.1 is an alkyl group, Z is not a hydrogen atom, a halogen atom nor a trifluoromethyl group, and (2) that when Q is ##STR4## wherein A is a nitrogen atom and Y.sub.1 is a trifluoromethyl group, Y.sub.2 is other than a hydrogen atom.

摘要翻译： 具有下式的N-苯甲酰脲化合物：其中X是氢原子，卤素原子或硝基，n是1至3的整数，Q是＆lt; IMAGE＆gt; 其中Y1是未取代或取代的烷基，或其烷基部分被未取代或取代的烷氧基或烷氧基羰基，Y2是氢原子，卤素原子，硝基，未取代或取代的烷基或烷氧基 或其烷基部分为未取代或取代的烷氧基羰基，Z为氢原子，卤素原子，三氟甲基或硝基，A和B各自为= CH-或氮原子，条件是A和 B是= CH-，另一个是氮原子，条件是（1）当Q是 + TR 时，当X是氢原子且Y1是烷基时，Z是 不是氢原子，卤素原子或三氟甲基，和（2）当Q是氮时，其中A是氮原子，Y 1是三氟甲基 堆，Y2不是氢原子。

公开(公告)号：US4845093A

公开(公告)日：1989-07-04

申请号：US111080

申请日：1987-10-19

申请人： Takahiro Haga ,  Nobutoshi Yamada ,  Hideo Sugi ,  Toru Koyanagi ,  hiroshi Okada

发明人： Takahiro Haga ,  Nobutoshi Yamada ,  Hideo Sugi ,  Toru Koyanagi ,  hiroshi Okada

IPC分类号： A61K31/50 ,  A61P35/00 ,  C07D237/14

CPC分类号： C07D237/14 ,  A61K31/50

摘要： An N-benzoyl-N'-pyridazinyloxyphenyl urea compound having the formula: ##STR1## wherein each of X.sub.1 and X.sub.2 is a hydrogen atom, a halogen atom or a nitro group, Y is a hydrogen atom, a halogen atom or a methyl group which may be substituted by fluorine, and Z is a hydrogen atom, a halogen atom or a trifluoromethyl group, provided that when X.sub.1 is a hydrogen atom and X.sub.2 is a hydrogen atom or a halogen atom, Y is a methyl group which may be substituted by fluorine and/or Z is a hydrogen atom or a trifluoromethyl group. The compound is useful as an active ingredient for an antitumorous composition.

摘要翻译： 具有下式的N-苯甲酰基-N'-哒嗪氧基苯基脲化合物：其中X1和X2各自为氢原子，卤素原子或硝基，Y为氢原子，卤素原子或 可以被氟取代的甲基，Z是氢原子，卤素原子或三氟甲基，条件是当X1为氢原子，X2为氢原子或卤素原子时，Y为甲基， 可以被氟取代，和/或Z是氢原子或三氟甲基。 该化合物可用作抗肿瘤组合物的活性成分。

公开(公告)号：US5102884A

公开(公告)日：1992-04-07

申请号：US554449

申请日：1990-07-19

申请人： Takahiro Haga ,  Nobutoshi Yamada ,  Hideo Sugi ,  Toru Koyanagi ,  Hiroshi Okada

发明人： Takahiro Haga ,  Nobutoshi Yamada ,  Hideo Sugi ,  Toru Koyanagi ,  Hiroshi Okada

IPC分类号： A61K31/505 ,  C07C237/42 ,  C07C275/46 ,  C07C311/31 ,  C07D239/34 ,  C07D401/12 ,  C07D403/12 ,  C07D413/12 ,  C07D417/12

CPC分类号： C07D239/34 ,  C07C237/42 ,  C07C311/31

摘要： A substituted benzoylurea compound of the formula (I): ##STR1## wherein R.sup.1 is a hydrogen atom, a halogen atom or a nitro group, each of R.sup.2 and R.sup.3 is a hydrogen atom, an alkyl group, --COR.sup.6 (wherein R.sup.6 is an alkyl group or an alkoxy group) or --SO.sub.2 R.sup.6 (wherein R.sup.6 is as defined above), or R.sup.2 and R.sup.3 may form together with the adjacent nitrogen atom a heterocyclic ring, R.sup.4 is a halogen atom, a substituted or unsubstituted alkyl group, a substituted or unsubstituted alkoxy group, a substituted or unsubstituted alkylthio group or a nitro group, and R.sup.5 is a halogen atom, a nitro group or a substituted or unsubstituted alkyl group, or its salt.

公开(公告)号：US4987135A

公开(公告)日：1991-01-22

申请号：US324559

申请日：1989-03-16

申请人： Takahiro Haga ,  Nobutoshi Yamada ,  Hideo Sugi ,  Toru Koyanagi ,  Hiroshi Okada

发明人： Takahiro Haga ,  Nobutoshi Yamada ,  Hideo Sugi ,  Toru Koyanagi ,  Hiroshi Okada

IPC分类号： C07D295/12 ,  A61K31/50 ,  A61K31/505 ,  A61P35/00 ,  C07C257/08 ,  C07C275/54 ,  C07C313/34 ,  C07C323/44 ,  C07C327/58 ,  C07C329/04 ,  C07C381/04 ,  C07C381/08 ,  C07D213/64 ,  C07D213/81 ,  C07D237/14 ,  C07D239/34 ,  C07D295/155 ,  C07D401/12 ,  C07F9/24 ,  C07F9/6512

CPC分类号： C07D213/64 ,  C07C257/08 ,  C07C327/58 ,  C07D237/14 ,  C07D239/34 ,  C07D295/155 ,  C07D401/12 ,  C07F9/65127 ,  C07C2101/08 ,  C07C2101/14

摘要： A substituted benzene derivative represented by a formula: ##STR1## where A represents: ##STR2## wherein X is a hydrogen atom, a halogen atom or a nitro group, R.sup.1 is --X.sup.1 Z.sup.1 (X.sup.1 is an oxygen atom or a sulfur atom and Z.sup.1 is a substituted or unsubstituted alkyl group, a substituted or unsubstituted alkenyl group, a substituted or unsubstituted alkynyl group, a substituted or unsubstituted aryl group or a substituted or unsubstituted heteroaryl group), --COZ.sup.1 group (Z.sup.1 is as defined above), ##STR3## group (Z.sup.1 is as defined above, Z.sup.2 is --CO.sub.2 Z.sup.3 wherein Z.sup.3 is the same as Z.sup.1, or --SO.sub.2 Z.sup.3 wherein Z.sup.3 is as defined above and n is 0 or 1), ##STR4## (Z.sup.1 and Z.sup.3 are as defined above) or ##STR5## (X.sup.2, X.sup.3 and X.sup.4 are, respectively, an oxygen atom or a sulfur atom and Z.sup.4 and Z.sup.5 are the same as Z.sup.1), and R.sup.3 is a nitro group or ##STR6## (R.sup.4 and R.sup.5 are, respectively, an alkyl group, or they may form a heterocyclic group together with the adjacent nitrogen atom), or ##STR7## wherein X and R.sup.3 are as defined above and R.sup.2 is --X.sup.1 Z.sup.1 (X.sup.1 and Z.sup.1 are as defined above); Y is a halogen atom, a substituted or unsubstituted alkyl group, a substituted or unsubstituted alkoxy group, a substituted or unsubstituted alkylthio group, a nitro group or ##STR8## (R.sup.6 and R.sup.7 are, respectively, a substituted or unsubstituted alkyl group); R is ##STR9## (R.sup.8 is the same as Y and q is an integer of 1 to 4), ##STR10## (R.sup.8 is as defined above, and r is an integer of 1 to 3) or ##STR11## (R.sup.8 and r are defined above); and m is an integer, of 1 to 4, or its salt.

公开(公告)号：US4677111A

公开(公告)日：1987-06-30

申请号：US782570

申请日：1985-10-01

申请人： Takahiro Haga ,  Nobutoshi Yamada ,  Hideo Sugi ,  Toru Koyanagi ,  Hiroshi Okada

发明人： Takahiro Haga ,  Nobutoshi Yamada ,  Hideo Sugi ,  Toru Koyanagi ,  Hiroshi Okada

IPC分类号： C07D213/64 ,  A61K31/44 ,  A61K31/4418 ,  A61K31/50 ,  A61K31/505 ,  A61P35/00 ,  C07D213/643 ,  C07D237/14 ,  C07D239/34 ,  C07D237/12 ,  C07D239/30

CPC分类号： C07D213/643 ,  C07D237/14 ,  C07D239/34

摘要： An N-benzoyl-N'-(3-nitrophenyl) urea compound having the formula ##STR1## wherein each of X.sub.1 and X.sub.2 is a hydrogen atom, a halogen atom, a trifluoromethyl group or a nitro group, and Y is ##STR2## (wherein R is a hydrogen atom, a halogen atom or a tirfluoromethyl group), provided that when Y is ##STR3## X.sub.1 and/or X.sub.2 is a nitro group. The compound is useful as an active ingredient of an antitumorous composition.

摘要翻译： 具有式“IMAGE”的N-苯甲酰基-N' - （3-硝基苯基）脲化合物，其中X1和X2各自为氢原子，卤素原子，三氟甲基或硝基，Y为 （其中R是氢原子，卤素原子或三氟甲基），条件是当Y是X 1和/或X 2是硝基时。 该化合物可用作抗肿瘤组合物的活性成分。

公开(公告)号：US4677110A

公开(公告)日：1987-06-30

申请号：US741134

申请日：1985-06-04

申请人： Takahiro Haga ,  Nobutoshi Yamada ,  Hideo Sugi ,  Toru Koyanagi ,  Hiroshi Okada

发明人： Takahiro Haga ,  Nobutoshi Yamada ,  Hideo Sugi ,  Toru Koyanagi ,  Hiroshi Okada

IPC分类号： A61K31/17 ,  A61K31/505 ,  A61P35/00 ,  C07D239/34 ,  C07D239/30

CPC分类号： C07D239/34

摘要： N-benzoyl-N'-pyrimidinyloxyphenyl urea compounds having the formula: ##STR1## wherein X represents a hydrogen atom, a halogen atom, a nitro group or a trifluoromethyl group and Z represents a hydrogen atom or a halogen atom, are useful as active ingredients of antitumorous compositions.

摘要翻译： 具有下式的N-苯甲酰基-N'-嘧啶氧基苯基脲化合物：其中X表示氢原子，卤素原子，硝基或三氟甲基，Z表示氢原子或卤素原子，可用作活性 抗肿瘤成分的成分。

公开(公告)号：US4849425A

公开(公告)日：1989-07-18

申请号：US824088

申请日：1986-01-30

申请人： Nobuo Kondo ,  Tsunetaka Nakajima ,  Masahiro Watanabe ,  Kazumasa Yokoyama ,  Tadakazu Suyama ,  Takahiro Haga ,  Nobutoshi Yamada ,  Hideo Sugi ,  Toru Koyanagi

发明人： Nobuo Kondo ,  Tsunetaka Nakajima ,  Masahiro Watanabe ,  Kazumasa Yokoyama ,  Tadakazu Suyama ,  Takahiro Haga ,  Nobutoshi Yamada ,  Hideo Sugi ,  Toru Koyanagi

IPC分类号： C07C273/00 ,  A61K9/00 ,  A61K9/02 ,  A61K9/20 ,  A61K9/48 ,  A61K31/44 ,  A61K31/505 ,  A61K47/10 ,  A61K47/40 ,  A61K47/44 ,  C07D239/34

CPC分类号： A61K9/02 ,  A61K31/44 ,  A61K31/505 ,  A61K47/10 ,  A61K47/40 ,  A61K47/44 ,  A61K9/0019 ,  A61K9/2013 ,  A61K9/4858 ,  C07D239/34 ,  Y10S514/946

摘要： A pharmaceutical composition comprises a benzoyl urea compound having the formula: ##STR1## wherein X is a nitro group, Y is a chlorine atom, Z.sub.2 is a hydrogen atom, Z.sub.1 is a halogen atom, and A is a nitrogen atom, and at least one member selected from the group consisting of a cyclodextrin, a polyethylene glycol and a refined oil.

公开(公告)号：US4727077A

公开(公告)日：1988-02-23

申请号：US823521

申请日：1986-01-29

申请人： Takahiro Haga ,  Nobutoshi Yamada ,  Hideo Sugi ,  Toru Koyanagi ,  Nobuo Kondo ,  Tsunetaka Nakajima ,  Masahiro Watanabe ,  Kazumasa Yokoyama

发明人： Takahiro Haga ,  Nobutoshi Yamada ,  Hideo Sugi ,  Toru Koyanagi ,  Nobuo Kondo ,  Tsunetaka Nakajima ,  Masahiro Watanabe ,  Kazumasa Yokoyama

IPC分类号： C07C273/00 ,  A61K9/00 ,  A61K9/02 ,  A61K9/20 ,  A61K9/48 ,  A61K31/44 ,  A61K31/505 ,  A61K47/10 ,  A61K47/40 ,  A61K47/44 ,  C07D239/34 ,  C07D251/22 ,  A61K31/53

CPC分类号： A61K9/02 ,  A61K31/44 ,  A61K31/505 ,  A61K47/10 ,  A61K47/40 ,  A61K47/44 ,  A61K9/0019 ,  A61K9/2013 ,  A61K9/4858 ,  C07D239/34 ,  Y10S514/946

摘要： A benzoyl urea compound having the formula: ##STR1## wherein A is a bromine atom or a chlorine atom.

摘要翻译： 具有下式的苯甲酰脲化合物：其中A是溴原子或氯原子。

公开(公告)号：US5098907A

公开(公告)日：1992-03-24

申请号：US469054

申请日：1990-01-23

申请人： Nobuo Kondo ,  Masahiro Kikuchi ,  Tsunetaka Nakajima ,  Masahiro Watanabe ,  Kouichi Yamauchi ,  Takahiro Haga ,  Nobutoshi Yamada ,  Hideo Sugi ,  Toru Koyanagi

发明人： Nobuo Kondo ,  Masahiro Kikuchi ,  Tsunetaka Nakajima ,  Masahiro Watanabe ,  Kouichi Yamauchi ,  Takahiro Haga ,  Nobutoshi Yamada ,  Hideo Sugi ,  Toru Koyanagi

IPC分类号： A61K9/14 ,  A61K31/44 ,  A61K31/505 ,  A61K47/14 ,  A61K47/26 ,  A61P35/00

CPC分类号： A61K9/14 ,  A61K31/44 ,  A61K31/505 ,  A61K47/14 ,  A61K47/26 ,  Y10S514/975

摘要： A powdery pharmaceutical composition comprising a benzoyl urea compound of the formula: ##STR1## wherein X is a halogen atom or a nitro group, Y is a hydrogen atom, a halogen atom, a nitro group or a trifluoromethyl group, Z.sub.1 is a halogen atom or a trifluoromethyl group, Z.sub.2 is a hydrogen atom or a halogen atom, and A is CH or a nitrogen atom, as an active ingredient, a nonionic surfactant as a dispersant, at least one member selected from the group consisting of sugar, sugar-alcohol and a nonionic surfactant as a disintegrant, and anhydrous silicic acid as a fluidizer.

公开(公告)号：US4983605A

公开(公告)日：1991-01-08

申请号：US110284

申请日：1987-10-20

申请人： Nobuo Kondo ,  Masahiro Kikuchi ,  Tsunetaka Nakajima ,  Masahiro Watanabe ,  Kazumasa Yokoyama ,  Takahiro Haga ,  Nobutoshi Yamada ,  Hideo Sugi ,  Toru Koyanagi

发明人： Nobuo Kondo ,  Masahiro Kikuchi ,  Tsunetaka Nakajima ,  Masahiro Watanabe ,  Kazumasa Yokoyama ,  Takahiro Haga ,  Nobutoshi Yamada ,  Hideo Sugi ,  Toru Koyanagi

IPC分类号： A61K9/14 ,  A61K9/19 ,  A61K31/44 ,  A61K31/50 ,  A61K31/505 ,  A61K47/14 ,  A61K47/26

CPC分类号： A61K31/505 ,  A61K31/44 ,  A61K31/50 ,  A61K9/145 ,  A61K9/146 ,  A61K9/19 ,  A61K47/14 ,  A61K47/26 ,  Y10S514/961 ,  Y10S514/964

摘要： A pharmaceutical composition comprising a benzoyl urea compound (A) selected from the group consisting of a benzoyl urea compound (I) having the formula: ##STR1## wherein X is a halogen atom, a nitro group or a trifluoromethyl group, provided that when Y is a nitro group, X is a halogen atom or a nitro group, Y is a hydrogen atom, a halogen atom, a nitro group or a trifluoromethyl group, Z.sub.1 is a halogen atom or a trifluoromethyl group, Z.sub.2 is a hydrogen atom or a halogen atom, and A is a .dbd.CH-- group or a nitrogen atom, and a benzoyl urea compound (II) having the formula: ##STR2## wherein each of X.sub.1 and X.sub.2 is a hydrogen atom, a halogen atom or a nitro group, provided that when Y is a nitro group, X.sub.1 is a hydrogen atom, Y is a hydrogen atom, a halogen atom, a nitro group or a trifluoromethyl group, and Z is a hydrogen atom, a halogen atom or a trifluoromethyl group, as an active ingredient; a nonionic surfactant as a dispersant; and at least one member selected from the group consisting of a saccharide, a saccharide alcohol, silicic anhydride and a nonionic surfactant, as a disintegrator.

摘要翻译： 提供一种药物组合物，其包含选自具有下式的苯甲酰脲化合物（I）的苯甲酰脲化合物（A）：其中X为卤素原子，硝基或三氟甲基，其提供 当Y为硝基时，X为卤原子或硝基，Y为氢原子，卤原子，硝基或三氟甲基，Z1为卤原子或三氟甲基，Z2为氢 原子或卤素原子，A为= CH-基或氮原子，和具有下式的苯甲酰脲化合物（II）：其中X1和X2各自为氢原子，卤素 原子或硝基，条件是当Y为硝基时，X 1为氢原子，Y为氢原子，卤素原子，硝基或三氟甲基，Z为氢原子，卤素原子或 三氟甲基作为活性成分; 作为分散剂的非离子表面活性剂; 和选自糖，糖醇，硅酸酐和非离子表面活性剂的至少一种作为崩解剂。