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    ヘテロ６員環化合物及びその用途
    91.
    发明申请
    ヘテロ６員環化合物及びその用途 审中-公开
    六元杂环化合物及其用途

    公开(公告)号：WO2006080323A1

    公开(公告)日：2006-08-03

    申请号：PCT/JP2006/301093

    申请日：2006-01-25

    Applicant: 旭化成ファーマ株式会社 ,  正田 基 ,  石津谷 俊則

    Inventor： 正田 基 ,  石津谷 俊則

    IPC: C07D237/04 ,  A61K31/50 ,  A61P1/02 ,  A61P19/00 ,  A61P19/02 ,  A61P19/08 ,  A61P19/10 ,  A61P29/00 ,  A61P43/00

    CPC classification number: C07D237/04

    Abstract: A compound that can be used as a pharmaceutical active ingredient effective in prevention and/or treatment of osteoporosis, a bone disease such as fracture, and further, glaucoma or ulcerative colitis, and is represented by the general formula (I): [Chemical formula 1] (I) [wherein T represents an oxygen atom or the like; V represents CH 2 or the like; R 01 to R 04 represent a hydrogen atom or the like; A represents a linear alkylene group or a linear alkenylene group having 2 to 8 carbon atoms or the like; D represents a carboxyl group or the like; X represents an ethylene group, a trimethylene group or the like; E represents a -CH(OH)- group or the like; and W represents a -U 1 -(R W1 )(R W2 )-U 2 -U 3 group (wherein U 1 represents a single bond or an alkylene group having 1 to 4 carbon atoms or the like; R W1 and R W2 represent a hydrogen atom or the like; U 2 represents a single bond, an alkylene group having 1 to 4 carbon atoms or the like; and U 3 represents an alkyl group having 1 to 8 carbon atoms or the like) or a residue of a carbocyclic or heterocyclic compound]; or a salt thereof.

    Abstract translation: 可用作有效预防和/或治疗骨质疏松，骨疾病如骨折，以及进一步的青光眼或溃疡性结肠炎的药物活性成分的化合物，并且由通式（I）表示：[化学式 1]（I）[其中T表示氧原子等; V表示CH 2 2等; R 01与R 04代表氢原子等; A表示直链亚烷基或碳原子数2〜8的直链亚烯基等; D表示羧基等; X表示亚乙基，三亚甲基等; E表示-CH（OH） - 基等; W表示-U 1 - （R W1）（R W2）-O 2 - 其中U 1表示单键或碳原子数1〜4的亚烷基等; R 1，W 2，R SUP， > W 2表示氢原子等; U 2表示单键，碳原子数为1〜4的亚烷基等，U 3 >表示碳原子数1〜8的烷基等）或碳环或杂环化合物的残基]; 或其盐。

    THERAPEUTIC AMIDE DERIVATIVES
    93.
    发明申请
    THERAPEUTIC AMIDE DERIVATIVES 审中-公开
    治疗酰胺衍生物

    公开(公告)号：WO2005080317A2

    公开(公告)日：2005-09-01

    申请号：PCT/IB2005/000258

    申请日：2005-02-01

    Applicant: PFIZER JAPAN, INC. ,  PFIZER INC. ,  KAWAI, Makoto ,  KAWAMURA, Mitsuhiro ,  SAKURADA, Isao ,  MORITA, Asato

    Inventor： KAWAI, Makoto ,  KAWAMURA, Mitsuhiro ,  SAKURADA, Isao ,  MORITA, Asato

    IPC: C07C235/00

    CPC classification number: C07C235/48 ,  C07C2601/14 ,  C07D207/34 ,  C07D209/34 ,  C07D213/64 ,  C07D213/81 ,  C07D213/82 ,  C07D215/227 ,  C07D215/48 ,  C07D231/14 ,  C07D231/56 ,  C07D233/90 ,  C07D235/26 ,  C07D237/04 ,  C07D237/24 ,  C07D249/04 ,  C07D263/38 ,  C07D277/68 ,  C07D303/22 ,  C07D309/06 ,  C07D317/72 ,  C07D401/12 ,  C07D405/06 ,  C07D405/12

    Abstract: The present invention relates to compounds of the formula (I): or a pharmaceutically acceptable salt or solvate thereof, wherein: A and B independently represent CH 2 or O, with the proviso that A and B are not simultaneously O; Cy represents one of the following Formula (II) optionally substituted by one to three groups selected from hydroxy, halogen, C 1-6 alkyl, C 1-6 alkoxy, C 1-6 haloalkyl, C 1-6 alkylamino and amino; R 1 and R 2 are independently selected from hydroxy, halogen, C 1-6 alkyl, C 1-6 alkoxy, C 1-6 haloalkyl and C 3-8 cycloalkyl; n represents an integer from 0-4; X is hydrogen, hydroxy, halogen or C 1-6 alkoxy; Y is oxy, thio, a 1-4 membered alkylene, a 2-4 membered alkylene ether, 2-4 membered alkylene thioether or an oxyethyleneoxy group, optionally substituted by 1 to 4 groups independently selected from hydroxy, halogen, C 1-6 alkyl, C 1-6 alkoxy and C 1-6 haloalkyl; Z is CH or N; and p represents an integer from 0-5 when Z is CH or 0-4 when Z is N; when p represents 2 or more, two of R 2 s may be taken together with the carbon atoms to which they are attached to form a 5-8 membered cycloalkyl ring to processes for the preparation of, intermediates used in the preparation of, compositions containing such compounds and the uses of such compounds as antagonists of the NMDA NR2B receptor.

    Abstract translation: 本发明涉及式（I）化合物或其药学上可接受的盐或溶剂化物，其中：A和B独立地表示CH 2或O，条件是A和B不同时为O; Cy表示任选被一至三个选自羟基，卤素，C 1-6烷基，C 1-6烷氧基，C 1-6卤代烷基，C 1-6烷基氨基和氨基的基团取代的下式（II）之一。 R 1和R 2独立地选自羟基，卤素，C 1-6烷基，C 1-6烷氧基，C 1-6卤代烷基和C 3-8环烷基; n表示0-4的整数; X是氢，羟基，卤素或C 1-6烷氧基; Y是氧基，硫代，1-4元亚烷基，2-4元亚烷基醚，2-4元亚烷基硫醚或氧化乙烯氧基，任选被1至4个独立地选自羟基，卤素，C 1-6烷基， C 1-6烷氧基和C 1-6卤代烷基; Z是CH或N; 当Z为CH时，p表示0-5的整数，Z为N时为0〜4的整数。 当p表示2或更多时，R 2中的两个可以与它们所连接的碳原子一起形成5-8元环烷基环，以制备用于制备中间体的中间体， 含有这些化合物的组合物以及这些化合物作为NMDA NR2B受体的拮抗剂的用途。

    ANTIBACTERIAL AGENTS
    96.
    发明申请
    ANTIBACTERIAL AGENTS 审中-公开
    抗菌剂

    公开(公告)号：WO2004050638A1

    公开(公告)日：2004-06-17

    申请号：PCT/GB2003/005179

    申请日：2003-12-01

    Applicant: VERNALIS (OXFORD) LTD. ,  EAST, Stephen, Peter

    Inventor： EAST, Stephen, Peter

    IPC: C07D237/04

    CPC classification number: C07D405/12 ,  C07D231/04 ,  C07D237/04 ,  C07D401/06 ,  C07D405/06

    Abstract: Compounds of formula (I) have antibacterial activity; wherein Q represents a radical of formula -N(OH)CH(=O) or formula -C(=O)NH(OH); Y represents -C(=O)-, -C(=S)-, -S(=O)-, or -SO 2 -; R 1 represents hydrogen, C l -C 6 alkyl or C l -C 6 alkyl substituted by one or more halogen atoms, or, except when Q is a radical of formula -N(OH)CH(=O), a hydroxy, C l -C 6 alkoxy, C 1 -C 6 alkenyloxy, halogen, amino, C l -C 6 alkylamino, or di-( C l -C 6 alkyl)amino group; R 2 represents a substituted or unsubstituted C l -C 6 alkyl, C l -C 3 alkyl-O-C 1 -C 3 alkyl, C 1 -C 3 alkyl-S-C l -C 3 alkyl, cycloalkyl(C l -C 3 alkyl)-, aryl(C 1 -C 3 alkyl)-, heterocyclyl(C l -C 3 alkyl)-, or R 1 R 2 N-C 1 -C 3 alkyl group wherein R 1 represents hydrogen or C 1 -C 3 alkyl and R 2 represents C l -C 3 alkyl, or R 1 R 2 N- represents a cyclic amino group; R 3 and R 4 taken together with the nitrogen atoms to which they are respectively attached form a saturated heterocyclic ring of from 4 to 7 ring atoms, which may be fused to a second carbocyclic or heterocyclic ring, either of which rings may optionally be substituted; and A represents a primary, secondary or tertiary amino group or a group -R 5 , -OR 5 , wherein R 5 is a substituted or unsubstituted C 1 -C 6 alkyl, C 2 -C 6 alkenyl, C 2 -C 6 alkynyl, cycloalkyl, aryl, heterocyclyl, C l -C 3 alkyl-O-C 1 -C 3 alkyl, C l -C 3 alkyl-S-C l -C 3 alkyl, cycloalkyl(C l -C 3 alkyl)-, heterocyclic(C l -C 3 alkyl, aryl(C l -C 3 alkyl)-or R 1 R 2 N-C 1 -C 3 alkyl group wherein R 1 represents hydrogen or C l -C 3 alkyl and R 2 represents C l -C 3 alkyl, or R 1 R 2 N- represents a cyclic amino group.

    Abstract translation: 式（I）化合物具有抗菌活性; 其中Q表示式-N（OH）CH（= O）或式-C（= O）NH（OH）的基团; Y表示-C（= O） - ， - C（= S） - ， - S（= O） - 或-SO 2 - R 1表示氢，C 1 -C 6烷基或被一个或多个卤素原子取代的C 1 -C 6烷基，或除了当Q是式-N（OH）CH（= O）基团时，除羟基，C 1 -C 6烷氧基， C 1 -C 6烯氧基，卤素，氨基，C 1 -C 6烷基氨基或二 - （C 1 -C 6烷基）氨基; R 2表示取代或未取代的C 1 -C 6烷基，C 1 -C 3烷基-O-C 1 -C 3烷基，C 1 -C 3烷基-S C 1 -C 3烷基，环烷基（C 1 -C 3烷基） - ，芳基（C 1 -C 3烷基 ） - ，杂环基（C 1 -C 3烷基） - 或R 1 R 2 N-C 1 -C 3烷基，其中R 1表示氢或C 1 -C 3烷基，R 2表示C 1 -C 3烷基 或R 1 R 2 N-表示环状氨基; R3和R4与它们分别连接的氮原子一起形成4至7个环原子的饱和杂环，其可以与第二碳环或杂环稠合，其中任一个可以任选被取代; 并且A表示伯，仲或叔氨基或基团-R 5 -OR 5，其中R 5是取代或未取代的C 1 -C 6烷基，C 2 -C 6烯基，C 2 -C 6炔基，环烷基，芳基，杂环基， C 3烷基-O-C 1 -C 3烷基，C 1 -C 3烷基-S-C 1 -C 3烷基，环烷基（C 1 -C 3烷基） - ，杂环（C 1 -C 3烷基，芳基（C 1 -C 3烷基））或R 1 其中R 1表示氢或C 1 -C 3烷基，R 2表示C 1 -C 3烷基，或R 1 R 2表示环状氨基 组。

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