4-IMIDAZOLIN-2-ONE COMPOUNDS
    22.
    发明申请
    4-IMIDAZOLIN-2-ONE COMPOUNDS 审中-公开
    4-咪唑烷-2-酮化合物

    公开(公告)号:WO2004094404A1

    公开(公告)日:2004-11-04

    申请号:PCT/JP2004/005716

    申请日:2004-04-21

    Abstract: The present invention relates to a compound of the formula [I] wherein G 1 is an alkyl which is substituted by a halogen atom or an alkoxy, or a group of the formula [II] wherein ring B is benzene ring which may be substituted, etc., Q 1 and Q 2 may be the same or different, and each is hydrogen atom, a halogen atom or an alkyl, n is 0, 1, 2, 3 or 4, R 1 is hydrogen atom, an alkyl which may be substituted, a cycloalkyl which may be substituted, a phenyl which may be substituted, etc., Z 1 , Z 2 , Z 3 and Z 4 may be the same or different, and each is CH or N, provided that 3 or more of Z 1 , Z 2 , Z 3 and Z 4 should not be N at the same time, G 2 is hydrogen atom, -NR 3 R 4 , -OR 5 , etc., where R 3 to R 8 each is independently hydrogen atom, an alkyl which may be substituted, an alkenyl, an alkynyl, etc., or a pharmaceutically acceptable salt thereof.

    Abstract translation: 本发明涉及式[I]的化合物,其中G 1是被卤素原子或烷氧基取代的烷基或式[II]的基团,其中环B是苯环,其可以是 取代等,Q 1和Q 2可以相同或不同,各自为氢原子,卤素原子或烷基,n为0,1,2,3或4,R 1为 Z可以是氢原子,可以被取代的烷基,可被取代的环烷基,可被取代的苯基等,Z 1,Z 2,Z 3和Z 4可以是 相同或不同,并且各自为CH或N,条件是Z 1,Z 2,Z 3和Z 4中的3个或更多个不应同时为N,G 2为 氢原子,-NR 3 R 4,-OR 5等,其中R 3至R 8各自独立地为氢原子,可被取代的烷基,烯基,炔基 等,或其药学上可接受的盐。

    A PYRAZOLOPYRIMIDINE COMPOUND AND A PROCESS FOR PREPARING THE SAME

    公开(公告)号:WO2004064721A3

    公开(公告)日:2004-08-05

    申请号:PCT/JP2004/000617

    申请日:2004-01-23

    Abstract: The present invention provides a novel pyrazolopyrimidine compound of the formula [I]: wherein R' is (A) a substituted aryl group, (B) an optionally substituted nitrogen-containing aliphatic heteromonocyclic group, (C) a substituted cyclo-lower alkyl group, (D) an optionally substituted amino group, or (E) a substituted heteroaryl group, R 2 is (a) an optionally substituted heteroaryl group or (b) an optionally substituted aryl group, Y is a single bond, a lower alkylene group or a lower alkenylene group, Z is a group of the formula: -CO-, -CH2-, -S02- or a group of the formula[II]: Q is a lower alkylene group, and q is an integer of 0 or 1 or a pharmaceutically acceptable sait thereof, which has a small conductance potassium channel (SK channel) blocking activity and is useful as a medicament and a process for preparing the same.

    PROCESS FOR PREPARING 9-HYDROXYELLIPTICINE
    25.
    发明申请
    PROCESS FOR PREPARING 9-HYDROXYELLIPTICINE 审中-公开
    制备9-羟基尿嘧啶的方法

    公开(公告)号:WO1997046559A1

    公开(公告)日:1997-12-11

    申请号:PCT/JP1997001825

    申请日:1997-05-29

    CPC classification number: C07D471/04 C07D209/88

    Abstract: A process for preparing 9-hydroxyellipticine, or salt thereof, which comprises treating acetal compound (I): wherein R is alkyl or aryl, R is lower alkyl or aryl, R and R are the same or different and each are substituted or unsubstituted lower alkyl, or both may combine each other at their termini to form substituted or unsubstituted lower alkylene, or a corresponding aldehyde thereof, with an acid, to give 9-hydroxyellipticine in a single step, and if necessary, converting the resulting 9-hydroxyellipticine into a salt thereof. These compounds are useful as an antitumor agent or an intermediate for preparing other medicaments.

    Abstract translation: 一种制备9-羟基椭圆体或其盐的方法,其包括处理缩醛化合物(I):其中R 1为烷基或芳基,R 2为低级烷基或芳基,R 3和R 4为 各自为取代或未取代的低级烷基,或两者可以在其末端彼此结合形成取代或未取代的低级亚烷基,或其相应的醛与酸,以在单一步骤中得到9-羟基乙基 ,并且如果需要,将所得的9-羟基乙基吡啶转化为其盐。 这些化合物可用作抗肿瘤剂或制备其它药物的中间体。

    2-OXOINDOLINE DERIVATIVE
    26.
    发明申请
    2-OXOINDOLINE DERIVATIVE 审中-公开
    2-氧杂吲哚衍生物

    公开(公告)号:WO1995014668A1

    公开(公告)日:1995-06-01

    申请号:PCT/JP1994001990

    申请日:1994-11-25

    Abstract: A 2-oxoindoline derivative represented by general formula (I) and a pharmacologically acceptable salt thereof, wherein ring A represents (un)substituted benzene; R represents hydrogen, cycloalkyl, aryl, nitrogenous heterocycle, oxygenous heterocycle, sulfurous heterocycle, heterocycle containing nitrogen and oxygen, heterocycle containing nitrogen and sulfur, lower alkoxy, carboxy, cyano, lower alkylthio, lower alkylsulfinyl, lower alkylsulfonyl, oxiranyl, or 2-(lower alkylthio)-1-hydroxyethyl; R represents aryl, a group represented by formula (a), (un)substituted nitrogenous heteromonocycle, (un)substituted nitrogenous heterobicycle, a group represented by formula (b), (wherein n represnts 1 or 2), oxygenous heterocycle, sulfurous heterocycle, heterocyle containing nitrogen and oxygen or heterocycle containing nitrogen and sulfur; R represents (un)substituted lower alkyl; Q represents a single bond or lower alkylene; and Y represents a single bond, lower alkylene or lower alkinylene.

    Abstract translation: 由通式(I)表示的2-氧代二氢吲哚衍生物及其药理学上可接受的盐,其中环A表示(未)取代的苯; R 1表示氢,环烷基,芳基,含氮杂环,含氧杂环,亚硫杂环,含氮和氧的杂环,含氮和硫的杂环,低级烷氧基,羧基,氰基,低级烷硫基,低级烷基亚磺酰基,低级烷基磺酰基,环氧乙烷基, 或2-(低级烷硫基)-1-羟乙基; R 2表示芳基,由式(a)表示的基团,(un)取代的含氮异单环,(un)取代的含氮异双环,由式(b)表示的基团,(其中n表示1或2),氧杂环 ,亚硫杂环,含有氮和氧的杂环,或含有氮和硫的杂环; R 3表示(un)取代的低级烷基; Q表示单键或低级亚烷基; Y表示单键,低级亚烷基或低级亚烷基。

    PYRAZOLE COMPOUNDS HAVING CANNABINOID RECEPTOR (CB1) ANTAGONIZING ACTIVITY
    28.
    发明申请
    PYRAZOLE COMPOUNDS HAVING CANNABINOID RECEPTOR (CB1) ANTAGONIZING ACTIVITY 审中-公开
    具有CANNABINOID受体(CB1)拮抗活性的吡唑化合物

    公开(公告)号:WO2007046550A1

    公开(公告)日:2007-04-26

    申请号:PCT/JP2006/321446

    申请日:2006-10-20

    Abstract: The present invention relates to a pyrazole compound having potent CB1-antagonizing activity, having the following formula [I]: wherein R 1 and R 2 are the same or different and an optionally substituted aryl group etc., R 3 is an alkyl group etc., E is one of the following groups of the formula (i) to (iv): Q 1 is a single bond, an alkylene group or a group of the formula: -N(R 7 )-, R 7 is a hydrogen atom or an alkyl group, Q 2 is a single bond, an oxygen atom or an alkylene group, R 4 is a cycloalkyl group, a group of the formula: -N(R 5 )(R 6 ) etc., one of R 5 and R 6 is a hydrogen atom or an alkyl group and the other is an alkyl group, a group of the formula: -N(R 8 )(R 9 ) etc., D is an oxygen atom etc., R A1 is an amino group etc., R A2 is an optionally substituted aliphatic heterocyclic group, R is an alkyl group optionally substituted by one to three halogen atom(s) etc., one of R 8 and R 9 is a hydrogen atom or an alkyl group and the other is an alkyl group etc., or a pharmaceutically acceptable salt thereof.

    Abstract translation: 本发明涉及具有强的CB1拮抗活性的吡唑化合物,具有下式[I]:其中R 1和R 2相同或不同,并且 任选取代的芳基等,R 3是烷基等,E是下列式(i)至(iv)中的一个:Q 1 是单键,亚烷基或下式基团-N(R 7) - ,R 7是氢原子或烷基, O 2是单键,氧原子或亚烷基,R 4是环烷基,下式的基团-N(R 5) SUP))(R 6)等,R 5和R 6之一是氢原子或烷基,另一个是 烷基,下式的基团-N(R 8)(R 9)等,D是氧原子等,R A1 是氨基等,R A2是任选取代的脂族杂环基,R是任选的烷基 被一至三个卤素原子取代,R 8和R 9之一是氢原子或烷基,另一个是烷基等 或其药学上可接受的盐。

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