序号 专利名 申请号 申请日 公开(公告)号 公开(公告)日 发明人
21 新規システイン化合物及びその塩 JP2014506256 2013-03-19 JPWO2013141264A1 2015-08-03 章良 浅井; 尚久 小郷; 潤一 澤田; 章弘 橋本
本発明は、Eg5阻害活性を有し、抗腫瘍剤として有用な新規化合物を提供することを目的とする。本発明は、下記一般式(I)[式(I)中、Aは、CH2、硫黄原子又は酸素原子、Rは、ハロゲン原子、C1−C6アルキル基、C1−C6アルコキシ基又はトリフルオロメチル基を示す。]で表される化合物又はその塩に関する。【化1】
22 Polymerizable monomer and polymer JP51936096 1995-12-18 JP4153031B2 2008-09-17 エバンス,リチャード・アレキサンダー; モード,グレアム; リザード,エジオ
23 Polycyclic alkaloid derivatives as Nmda receptor antagonist JP50603297 1996-07-12 JPH11509533A 1999-08-24 ディクシット,ディリップ,エム; ディマイオ,ジョン
(57)【要約】 次式(I) [式中、R 1はH、炭素原子数1ないし6のアルキル基、または炭素原子数6ないし12のアリール基であって所望により極性基で置換された基を表し、R 2およびR 3は独立してH、OH、炭素原子数1ないし6のアルキル基、−C(NH)−NH 2 、正帯電した基、または炭素原子数7ないし13のアラルキル基であって所望によりNH 2 、OH、炭素原子数1ないし6のアルキル基またはハロゲン原子で置換された基を表すか、またはR 2およびR 3は一緒になって所望によりヘテロ原子を組み入れる5ないし6員環を形成し、R 4はH、炭素原子数1ないし6のアルキル基、OR 6 、SR 6またはN(R 62を表し、ここでそれぞれのR 6は独立してH、炭素原子数1ないし3のアルキル基を表し、XはO、S、SO、SO 2 、N−R 5またはC−(R 52を表し、ここでそれぞれのR 5は独立してH、炭素原子数1ないし6のアルキル基、または炭素原子数7ないし13のアラルキル基であって所望により1個またはそれ以上のヘテロ原子で中断された基を表し、nは0ないし2の整数を表し、mは0ないし3の整数を表し、但し、XがCH 2を表すとき、R 1はCH 3を表さず、R 2およびR 3は双方ともHを表さず、R 4はOHを表さず、mは3を表さず、またnは0を表さない。 ]で表される多環式アルカロイド。 それはイオノトロピックNMDA(N−メチル−(D)−アスパラギン酸)受容体で拮抗薬として作用する。
24 新規システイン化合物及びその塩 JP2014506256 2013-03-19 JP5662618B2 2015-02-04 章良 浅井; 尚久 小郷; 潤一 澤田; 章弘 橋本
25 New heterocyclic compounds for the treatment of pain and their applications JP50610997 1996-07-12 JPH11509211A 1999-08-17 ディクシット,ディリップ,エム.; ディマイオ,ジョン
(57)【要約】 次式(I)で表される多環式アルカロイド: (式中、R 1はH、炭素原子数1ないし6のアルキル基または場合により極性基で置換された炭素原子数6ないし12のアリール基を表し、R 2およびR 3は独立してH、OH、炭素原子数1ないし6のアルキル基、−C(NH)−NH 2 、陽に荷電した基、または場合によりNH 2 、OH、炭素原子数1ないし6のアルキル基またはハロゲン原子で置換された炭素原子数7ないし13のアルアルキル基を表すか、またはR 2およびR 3は一緒になって場合により異原子を含む5ないし6員環を形成し、R 4はH、炭素原子数1ないし6のアルキル基、OR 6 、SR 6またはN(R 62を表し、各々のR 6は独立してH、炭素原子数1ないし3のアルキル基またはハロゲン原子を表し、XはO、S、SO、SO 2 、N−R 5またはC−(R 52を表し、各々のR 5は独立してH、炭素原子数1ないし6のアルキル基または1もしくはそれより多い異原子で場合により中断された炭素原子数7ないし13のアルアルキル基を表し、nは0ないし2の整数を表し、mは0ないし3の整数を表すが、ただし、XがCH 2である場合、R 1はCH 3ではなく、R 2およびR 3は両方Hではなく、R 4はOHではなく、mは3ではなく、そしてnは0ではない)。 痛みの処置のための上記化合物を含有する薬学的に許容され得る組成物。 本発明の化合物はアヘン剤受容体でアゴニストとして作用する。
26 Substituted pyridazones and herbicides containing said compound JP6615876 1976-06-08 JPS52289A 1977-01-05 ADORUFU FUITSUSHIERU; HANSUPEETERU HANZEN; UORUFUGANGU ROORU
27 NOVEL HETEROCYCLIC COMPOUNDS FOR THE TREATMENT OF PAIN AND USE THEREOF EP96921855.1 1996-07-12 EP0850234B1 2001-11-28 DIMAIO, John; DIXIT, Dilip M
Polycyclic alkaloids of formula (I), wherein R1 is H, C1-6 alkyl, or C6-12 aryl optionally substituted with polar groups; R2 and R3 are independently H, OH, C1-6 alkyl, -C(NH)-NH2, a positively charged group, or C7-13 aralkyl optionally substituted with NH2, OH, C1-6 alkyl, or halogen; or R2 and R3 together form a 5 to 6 member ring optionally incorporating a heteroatom; R4 is H, C1-6 alkyl, OR6, SR6 or N(R6)2, wherein each R6 is independently H, C1-3 alkyl, or halogen; X is O, S, SO, SO2, N-R5, or C-(R5)2, wherein each R5 is independently H, C1-6 alkyl, or C7-13 aralkyl optionally interrupted with one or more heteroatom; n is an integer from 0 to 2; m is an integer from 0 to 3; with the proviso that when X is CH2 then R1 is not CH3, R2 and R3 are not both H, R4 is not OH, m is not 3 and n is not 0. For the treatment of pain and pharmaceutically acceptable compositions comprising those compounds. The compounds of this invention act as agonists at the opiate receptor.
28 POLYCYCLIC ALCALOID-DERIVATIVES AS NMDA-RECEPTOR ANTAGONISTS EP96922703.2 1996-07-12 EP0840731B1 2001-10-10 DIMAIO, John; DIXIT, Dilip, M.
Polycyclic alkaloids of formula (I), wherein R1 is H, C1-6 alkyl, or C6-12 aryl optionally substituted with polar groups; R2 abd R3 are independently H, OH, C1-6 alkyl, -C(NH)-NH2, a positively charged group, or C7-13 aralkyl optionally substituted with NH2, OH, C1-6 alkyl, or halogen; or R2 and R3 together form a 5 to 6 member ring optionally incorporating a heteroatom; R4 is H, C1-6 alkyl, OR6, SR6 or N(R6)2, wherein each R6 is independently H, C1-3 alkyl; X is O, S, SO, SO2, N-R5, or C-(R5)2, wherein each R5 is independently H, C1-6 alkyl, or C7-13 aralkyl optionally interrupted with one or more heteroatom; n is an integer from 0 to 2; m is an integer from 0 to 3; with the proviso that when X is CH2 then R1 is not CH3, R2 and R3 are not both H, R4 is not OH, m is not 3 and n is not 0. That act as antagonists at the ionotropic NMDA (N-methyl-(D)-aspartic acid) receptor.
29 Procédé de synthèse d'hétérocycles à partir de complexes palladocycliques EP87111247.0 1987-08-04 EP0255715B1 1991-07-31 Pfeffer, Michel, Dr.; Maassarani, Figa; Dupont, Jairton
30 Tricyclic amine derivatives EP89200473.0 1989-02-27 EP0332246A1 1989-09-13 Rae, Duncan Robertson; Cairns, James

The present invention deals with dibenzo-oxocin-, dibenzo-thiocin-, dibenzo-azocin-and dibenzocyclo-octen­amine derivatives suitable for use as antipsychotic compounds without extra-pyrimidal side-effects.

31 POLYMERISABLE MONOMERS AND POLYMERS EP95941979.7 1995-12-18 EP0799220B1 2003-04-09 EVANS, Richard, Alexander; RIZZARDO, Ezio; MOAD, Graeme
Compounds of formulae (1a) and (1b), wherein R1 to R4 may be the same or different and are selected from hydrogen, halogen, optionally substituted alkyl, optionally substituted aryl, nitrile, hydroxy, alkoxy acyloxy and ester; or R?1 and R2 or R3 and R4¿ together form methylene; X is selected from sulfur, sulfoxide, sulfone and disulfide; Y is selected from sulfur, oxygen, N-H, N-alkyl, N-aryl, acyl and CR5R6 wherein R?5 and R6¿ are the same as R?1 to R4; and Z1 and Z2¿ are linking functionalites, with the proviso that when R1 to R4 are hydrogen and X and Y are sulfur in the compound of formula (1a), then Z1 is not -(CH¿2?)2- or -CH2-C(=CH2)-CH2-. Compounds of formula (1a) and (1b) are used to produce polymers, copolymers or block polymer to manufacture adhesives, dental compositions or optical lenses.
32 POLYCYCLIC ALCALOID-DERIVATIVES AS NMDA-RECEPTOR ANTAGONISTS EP96922703.0 1996-07-12 EP0840731A1 1998-05-13 DIMAIO, John; DIXIT, Dilip, M.
Polycyclic alkaloids of formula (I), wherein R1 is H, C1-6 alkyl, or C6-12 aryl optionally substituted with polar groups; R2 abd R3 are independently H, OH, C1-6 alkyl, -C(NH)-NH2, a positively charged group, or C7-13 aralkyl optionally substituted with NH2, OH, C1-6 alkyl, or halogen; or R2 and R3 together form a 5 to 6 member ring optionally incorporating a heteroatom; R4 is H, C1-6 alkyl, OR6, SR6 or N(R6)2, wherein each R6 is independently H, C1-3 alkyl; X is O, S, SO, SO2, N-R5, or C-(R5)2, wherein each R5 is independently H, C1-6 alkyl, or C7-13 aralkyl optionally interrupted with one or more heteroatom; n is an integer from 0 to 2; m is an integer from 0 to 3; with the proviso that when X is CH2 then R1 is not CH3, R2 and R3 are not both H, R4 is not OH, m is not 3 and n is not 0. That act as antagonists at the ionotropic NMDA (N-methyl-(D)-aspartic acid) receptor.
33 POLYMERISABLE MONOMERS AND POLYMERS EP95941979 1995-12-18 EP0799220A4 1998-04-15 EVANS RICHARD ALEXANDER; RIZZARDO EZIO; MOAD GRAEME
Compounds of formulae (1a) and (1b), wherein R1 to R4 may be the same or different and are selected from hydrogen, halogen, optionally substituted alkyl, optionally substituted aryl, nitrile, hydroxy, alkoxy acyloxy and ester; or R?1 and R2 or R3 and R4¿ together form methylene; X is selected from sulfur, sulfoxide, sulfone and disulfide; Y is selected from sulfur, oxygen, N-H, N-alkyl, N-aryl, acyl and CR5R6 wherein R?5 and R6¿ are the same as R?1 to R4; and Z1 and Z2¿ are linking functionalites, with the proviso that when R1 to R4 are hydrogen and X and Y are sulfur in the compound of formula (1a), then Z1 is not -(CH¿2?)2- or -CH2-C(=CH2)-CH2-. Compounds of formula (1a) and (1b) are used to produce polymers, copolymers or block polymer to manufacture adhesives, dental compositions or optical lenses.
34 POLYMERISABLE MONOMERS AND POLYMERS EP95941979.0 1995-12-18 EP0799220A1 1997-10-08 EVANS, Richard, Alexander; RIZZARDO, Ezio; MOAD, Graeme
Compounds of formulae (1a) and (1b), wherein R1 to R4 may be the same or different and are selected from hydrogen, halogen, optionally substituted alkyl, optionally substituted aryl, nitrile, hydroxy, alkoxy acyloxy and ester; or R?1 and R2 or R3 and R4¿ together form methylene; X is selected from sulfur, sulfoxide, sulfone and disulfide; Y is selected from sulfur, oxygen, N-H, N-alkyl, N-aryl, acyl and CR5R6 wherein R?5 and R6¿ are the same as R?1 to R4; and Z1 and Z2¿ are linking functionalites, with the proviso that when R1 to R4 are hydrogen and X and Y are sulfur in the compound of formula (1a), then Z1 is not -(CH¿2?)2- or -CH2-C(=CH2)-CH2-. Compounds of formula (1a) and (1b) are used to produce polymers, copolymers or block polymer to manufacture adhesives, dental compositions or optical lenses.
35 ARTHROPODICIDAL CARBOXANILIDES PCT/US9109172 1991-12-17 WO9212133A3 1992-10-15 HARRISON CHARLES RICHARD; KRANIS KEVIN THOMAS; STEVENSON THOMAS MARTIN
Compounds of formula (I), wherein Q, X, R?1, R2, R9¿ and Z are as defined in the text, including compositions containing said compounds and a method for using them to control arthropods.
QQ群二维码
意见反馈