CB.sub.2 Receptor agonist compounds

    公开(公告)号:US6013648A

    公开(公告)日:2000-01-11

    申请号:US995902

    申请日:1997-12-22

    摘要: The use of human CB.sub.2 receptor-specific agonists of formula (I) or (I') for preparing immunomodulating drugs is disclosed. In formulae (I) and (I'), R.sub.1 is a group selected from --CH.sub.2 CHR.sub.10 NR.sub.6 R.sub.11, --(CH.sub.2).sub.2 NR'.sub.6 R'.sub.11, --CHR.sub.9 CH.sub.2 NR'.sub.6 R'.sub.11, --(CH.sub.2).sub.n Z and --COR.sub.8 ; R'.sub.1 is a --CH.sub.2 CHR.sub.10 NR.sub.6 R.sub.11 or --(CH.sub.2).sub.2 NR'.sub.6 R'.sub.11 group; R.sub.2 and R'.sub.2 are hydrogen, halogen or C.sub.1-4 alkyl; R.sub.3 is hydrogen, C.sub.1-4 alkyl or a group selected from --CH.sub.2 CHR.sub.10 NR.sub.6 R.sub.11, --(CH.sub.2).sub.2 NR'.sub.6 R'.sub.11 and --COR.sub.8 ; R'.sub.3 is a .dbd.CR.sub.6 R.sub.8 group; R.sub.4 has one of the meanings given for R.sub.5 or is a --COR.sub.8 group; R.sub.5 is hydrogen, C.sub.1-4 alkyl, C.sub.1-4 alkoxy, a halogen atom, a CF.sub.3 group, an OCF.sub.3 group or C.sub.1-4 alkylthio; R'.sub.5 has one of the meanings given for R.sub.5 and is in the 5 or 6 position of the indene ring; R.sub.6 is hydrogen or C.sub.1-4 alkyl; R'.sub.6 is C.sub.1-4 alkyl; R.sub.7 has one of the meanings given for R.sub.5 or R.sub.7 and R.sub.9 together form a --Y--CH.sub.2 -- group attached to the indole ring in the 7 position by a group Y; R.sub.8 is phenyl substituted one to four times by a substituent selected from halogen, C.sub.1-4 alkyl or C.sub.1-4 alkoxy; a polycyclic ring selected from naphth-1-yl, naphth-2-yl, 1,2,3,4-tetrahydronaphth-1-yl, 1,2,3,4-tetrahydronaphth-5-yl, anthryl, benzofuryl, benzothien-2-yl, benzothien-3-yl, 2-, 3-, 4- or 8-quinolyl, said polycyclic rings optionally being substituted once or twice by a substituent selected from C.sub.1-4 alkyl, C.sub.1-4 alkoxy, C.sub.1-4 alkylthio, halogen, cyano, hydroxyl, trifluoromethyl and imidazol-1-yl; R.sub.10 and R.sub.11 together are a group selected from --CH.sub.2 --O--CH.sub.2 --CR.sub.12 R.sub.13 -- and --(CH.sub.2).sub.p --CR.sub.12 R.sub.13 --, wherein the carbon atom substituted by R.sub.12 and R.sub.13 is attached to the nitrogen atom; R'.sub.11 is C.sub.1-4 alkyl; or R'.sub.11 and R'.sub.6, taken together with the nitrogen atom to which they are attached, form a group selected from morpholin-4-yl, thiomorpholin-4-yl, piperidin-1-yl and pyrrolidin-1-yl; each of R.sub.12 and R.sub.13 is independently hydrogen or C.sub.1-4 alkyl; n is 2, 3, 4 or 5; p is 2 or 3; Z is a methyl group or a halogen atom; and Y is a methylene group or an oxygen atom.

    Dihydroperimidine squarylium compound and mixture of dihydroperimidine
squarylium compounds
    84.
    发明授权
    Dihydroperimidine squarylium compound and mixture of dihydroperimidine squarylium compounds 失效
    二氢嘧啶方酸化合物和二氢嘧啶方酸化合物的混合物

    公开(公告)号:US5959105A

    公开(公告)日:1999-09-28

    申请号:US10121

    申请日:1998-01-21

    摘要: A dihydroperimidine squarylium compound is represented by the formula (I): ##STR1## in which each of R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6, R.sup.7, R.sup.8, R.sup.9, R.sup.10, R.sup.11 and R.sup.12 independently is hydrogen, an alkyl group, a cycloalkyl group, an aryl group, an aralkyl group, an alkenyl group, an alkynyl group or an acyl group; R.sup.1 and R.sup.2, R.sup.3 and R.sup.4, R.sup.5 and R.sup.6, R.sup.7 and R.sup.8, R.sup.9 and R.sup.10 or R.sup.11 and R.sup.12 may be combined with each other to form a five- or six-membered nitrogen-containing heterocyclic ring; R.sup.2 and R.sup.3, R.sup.6 and R.sup.7 or R.sup.10 and R.sup.11 may be combined with each other to form a five- or six-membered aliphatic ring; and n is an integer of 1 to 6. The specification further discloses a mixture of dihydroperimidine squarylium compounds, an infrared absorbing sheet and a silver halide photographic material.

    摘要翻译: 二氢嘧啶方酸鎓化合物由式(I)表示:其中R1,R2,R3,R4,R5,R6,R7,R8,R9,R10,R11和R12各自独立地为氢,烷基,环烷基 基团,芳基,芳烷基,烯基,炔基或酰基; R 1和R 2,R 3和R 4,R 5和R 6,R 7和R 8,R 9和R 10或R 11和R 12可以彼此结合形成五元或六元含氮杂环; R2和R3,R6和R7或R10和R11可以彼此结合形成五元或六元脂肪环; 并且n为1至6的整数。该说明书还公开了二氢嘧啶方酸化合物,红外线吸收片和卤化银照相材料的混合物。

    Procedure for alkylation of imides
    85.
    发明授权
    Procedure for alkylation of imides 失效
    酰亚胺烷基化方法

    公开(公告)号:US5780645A

    公开(公告)日:1998-07-14

    申请号:US775800

    申请日:1996-12-31

    摘要: A process for the alkylation of imides wherein the imides are reacted with a dialkyl carbonate, in the liquid state, at a temperature of between 100.degree. C. and 250.degree. C. and at a pressure of between 0 and 60 atmospheres in the presence of a basic catalyst. The dialkyl carbonate reagents are not very toxic and are thermally stable and their use as alkylation agents makes it possible to produce waste products with a negligible saline content.

    摘要翻译: 用于烷基化酰亚胺的方法,其中所述酰亚胺与碳酸二烷基酯在液态下在100℃至250℃的温度和0至60个大气压的压力下在存在下进行反应 一个基本的催化剂。 碳酸二烷基酯试剂不是非常有毒的并且是热稳定的,并且它们作为烷基化剂的使用使得可以生产具有可忽略的盐水含量的废物。

    Tricyclic quinoxalinedione derivatives
    87.
    发明授权
    Tricyclic quinoxalinedione derivatives 失效
    三环喹喔啉二酮衍生物

    公开(公告)号:US5719152A

    公开(公告)日:1998-02-17

    申请号:US611973

    申请日:1996-03-06

    摘要: A tricyclic quinoxalinedione derivative represented by the formula 1: ##STR1## wherein X represents hydrogen, alkyl, halogen, cyano, trifluoromethyl, or nitro; R.sup.1 represents hydrogen, alkyl, cycloalkyl, or cycloalkylalkyl; G represents --CONR.sup.2 -- or --NR.sup.2 CO--, wherein R.sup.2 represents hydrogen or alkyl; J represents an acidic group or a group which is convertible thereto in vivo; E represents an basic group or a group which is convertible thereto in vivo; Y represents a single bond, alkylene, alkenylene, substituted alkylene, or Y.sup.1 --Q--Y.sup.2, wherein Y.sup.1 represents a single bond or alkylene, Y.sup.2 represents alkylene, and Q represents a heteroatom selected from oxygen or sulfur; Z represents alkylene, or a pharmaceutically acceptable salt thereof, these compounds are selective antagonists of glycine binding site of the NMDA receptor.

    摘要翻译: 由式1表示的三环喹喔啉二酮衍生物:其中X表示氢,烷基,卤素,氰基,三氟甲基或硝基; R1代表氢,烷基,环烷基或环烷基烷基; G表示-CONR2-或-NR2CO-,其中R2表示氢或烷基; J表示酸性基团或可在体内转化的基团; E表示可在体内转化的碱性基团或基团; Y表示单键,亚烷基,亚烯基,取代的亚烷基或Y1-Q-Y2,其中Y1表示单键或亚烷基,Y2表示亚烷基,Q表示选自氧或硫的杂原子; Z表示亚烷基或其药学上可接受的盐,这些化合物是NMDA受体的甘氨酸结合位点的选择性拮抗剂。

    Fused pyrrolocarbazoles
    90.
    发明授权
    Fused pyrrolocarbazoles 失效
    熔融吡咯并咔唑

    公开(公告)号:US5591855A

    公开(公告)日:1997-01-07

    申请号:US427160

    申请日:1995-04-24

    摘要: Disclosed herein are compounds referred to as "fused pyrrolocarbazoles" which possess a variety of functional activities. The disclosed compounds are represented by the following general formula: ##STR1## Methodologies for the synthetic production of fused pyrrolocarbazoles are also disclosed, as well as exemplary uses of the compounds.

    摘要翻译: 本文公开了具有各种功能活性的被称为“稠合吡咯并唑”的化合物。 所公开的化合物由以下通式表示:还公开了合成生产稠合吡咯并咔唑的方法,以及化合物的示例性用途。