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    Oxazolidinone derivatives with antibiotic activity
    1.
    发明授权
    Oxazolidinone derivatives with antibiotic activity 有权
    具有抗菌活性的恶唑烷酮衍生物

    公开(公告)号：US07141583B2

    公开(公告)日：2006-11-28

    申请号：US10258355

    申请日：2001-04-23

    申请人： Michael Barry Gravestock ,  Michael John Betts ,  Ian Richard Matthews ,  David Alan Griffin

    发明人： Michael Barry Gravestock ,  Michael John Betts ,  Ian Richard Matthews ,  David Alan Griffin

    IPC分类号： A61K31/4439 ,  A61K31/454 ,  C07D401/14

    CPC分类号： C07D231/12 ,  C07D233/56 ,  C07D249/08 ,  C07D413/06 ,  C07D413/14 ,  C07D417/14 ,  C07D491/10

    摘要： Compounds of the formula (I), or a pharmaceutically acceptable salt, or an in-vivo-hydrolysable ester thereof, wherein HET is an N-linked 5-membered heteroaryl ring, optionally substituted on a C atom by an oxo or thioxo group; and/or by 1 or 2 (1–4C)alkyl groups; and/or on an available nitrogen atom by (1–4C)alkyl; or HET is an N-linked 6-membered heteroaryl ring containing up to three nitrogen heteroatoms in total, optionally substituted on a C atom as above; Q is selected from, for example, Q1 R2 and R3 are independently hydrogen or fluoro; T is selected from a range of groups, for example, of formula (TC5) wherein Rc is, for example, R13CO—, R13SO2— or R13CS—; wherein R13 is, for example, optionally substituted (1–10C)alkyl or R14C(O)O(1–6C)alkyl wherein R14 is optionally substituted (1–10C)alkyl; are useful as antibacterial agents; and processes for their manufacture and pharmaceutical compositions containing them are described.

    摘要翻译： 式（I）化合物或其药学上可接受的盐或其体内可水解的酯，其中HET是通过氧代或硫代基团在C原子上取代的N-连接的五元杂芳基环; 和/或1或2（1-4C）烷基; 和/或在可用的氮原子上由（1-4C）烷基取代; 或HET是总共含有多达三个氮杂原子的N-连接的6-元杂芳基环，任选地如上所述在C原子上取代; Q选自例如Q1 R 2和R 3独立地是氢或氟; T选自例如式（TC5）的基团范围，其中R c是例如R 13 CO-，R 13 SO 2 - 或R 13 CS-; 其中R 13为例如任选取代的（1-10C）烷基或R 14 C（O）O（1-6C）烷基，其中R 14 任选取代的（1-10C）烷基; 作为抗菌剂是有用的; 并描述了其制造方法和含有它们的药物组合物。

    Immuno inhibitory pyrazolone compounds
    2.
    发明授权
    Immuno inhibitory pyrazolone compounds 有权

    公开(公告)号：US07816361B2

    公开(公告)日：2010-10-19

    申请号：US10577470

    申请日：2004-11-02

    申请人： Ian Richard Matthews

    发明人： Ian Richard Matthews

    IPC分类号： A61K31/496 ,  A61K31/4152 ,  A61K31/4155 ,  C07D231/08 ,  C07D401/14

    CPC分类号： C04B35/632 ,  C07D231/22 ,  C07D401/04 ,  C07D401/12 ,  C07D401/14 ,  C07D403/04 ,  C07D405/04 ,  C07D405/14 ,  C07D413/14

    摘要： Compounds of formula (IA) or (IB) are inhibitors of CD80 and useful in immunomodulation therapy: wherein Ar represents an optionally substituted monocyclic or bicyclic aromatic or heteroaromatic group having from 5 to 10 ring atoms; R1 and R2 independently represent H, or C1-C6 alkyl; R3 represents H; F; CI; Br, —NO2; —CN; C1-C6 alkyl optionally substituted by F or CI; or C1-C6 alkoxy optionally substituted by F; R4 represents a carboxylic acid group (—COOH) or an ester thereof, or —C(═O)NR6R7, —NR7C(═O)R6, —NR7C(═O)OR6, —NHC(═O)NR7R6 or —NHC(═S)NR7R6 wherein R6 represents H, or a radical of formula -(Alk)m-Q wherein m is 0 or 1, Alk is an optionally substituted divalent straight or branched C1-C12 alkylene, or C2-C12 alkenylene, or C2-C12 alkynylene radical or a divalent C3-C12 carbocyclic radical, any of which radicals may be interrupted by one or more —O—, —S— or —N(R8)— radicals wherein R8 represents H or C1-C4 alkyl, C3-C4 alkenyl, C3-C4 alkynyl, or C3-C6 cycloalkyl, and Q represents H; —CF3; —OH; —SH; —NR8R8 wherein each R8 may be the same or different, or form a ring when taken together with the nitrogen to which they are attached; an ester group; or an optionally substituted aryl, aryloxy, cycloalkyl, cycloalkenyl or heterocyclic group; and R7 represents H or C1-C6 alkyl; or when taken together with the atom or atoms to which they are attached R6 and R7 form a monocyclic heterocyclic ring having 5, 6 or 7 ring atoms; and X represents a bond or a divalent radical of formula -(Z)n-(Alk)- or -(Alk)-(Z)n- wherein Z represents —O—, —S— or —NH—, Alk is as defined in relation to R6 and n is 0 or 1.

    Process for preparing pyrrolidinones
    4.
    发明授权
    Process for preparing pyrrolidinones 失效
    制备吡咯烷酮的方法

    公开(公告)号：US5670656A

    公开(公告)日：1997-09-23

    申请号：US651181

    申请日：1996-05-24

    申请人： John Michael Cox ,  Kevin James Gillen ,  Russell Martin Ellis ,  Shaheen Khatoon Vohra ,  Stephen Christopher Smith ,  Ian Richard Matthews

    发明人： John Michael Cox ,  Kevin James Gillen ,  Russell Martin Ellis ,  Shaheen Khatoon Vohra ,  Stephen Christopher Smith ,  Ian Richard Matthews

    IPC分类号： C07D207/26 ,  C07D207/273 ,  C07D207/28

    CPC分类号： C07D207/273

    摘要： A process for the preparation of a compound of general formula II: ##STR1## wherein R.sup.1 is hydrogen, or C.sub.1 -C.sub.10 hydrocarbyl or heterocyclyl having 3 to 8 ring atoms, either of which may optionally be substituted; each R.sup.2, R.sup.3, R.sup.4 and R.sup.5 is independently hydrogen or C.sub.1 -C.sub.4 alkyl; A is an optionally substituted aromatic or heteroaromatic ring system; and R.sup.21 is hydrogen, halogen, OH or OCONHR.sup.1, wherein R.sup.1 is as defined above; the process comprising cyclizing a compound of general formula III: ##STR2## wherein A, R.sup.2, R.sup.3, R.sup.4, R.sup.5 and R.sup.21 are as defined in general formula II and R.sup.25 is a leaving group such as a halogen atom; under basic conditions.

    摘要翻译： 制备通式II化合物的方法：其中R 1是氢，或C 1 -C 10烃基或具有3至8个环原子的杂环基，其中任一个可任选地被取代; 每个R 2，R 3，R 4和R 5独立地是氢或C 1 -C 4烷基; A是任选取代的芳族或杂芳族环系; 并且R 21是氢，卤素，OH或OCONHR 1，其中R 1如上所定义; 该方法包括使通式III的化合物：其中A，R 2，R 3，R 4，R 5和R 21如通式II中所定义，R 25是离去基团如卤素原子; 在基本条件下

    Immuno Inhibitory Pyrazolone Compounds
    6.
    发明申请
    Immuno Inhibitory Pyrazolone Compounds 有权
    免疫抑制吡唑啉酮化合物

    公开(公告)号：US20100331342A1

    公开(公告)日：2010-12-30

    申请号：US12874280

    申请日：2010-09-02

    申请人： Ian Richard Matthews

    发明人： Ian Richard Matthews

    IPC分类号： A61K31/496 ,  C07D401/14 ,  A61K31/497 ,  A61K31/454 ,  C07D403/12 ,  C07D231/22 ,  A61K31/4152 ,  A61P37/02 ,  A61P19/02 ,  A61P11/06 ,  A61P3/10 ,  A61P25/28

    CPC分类号： C04B35/632 ,  C07D231/22 ,  C07D401/04 ,  C07D401/12 ,  C07D401/14 ,  C07D403/04 ,  C07D405/04 ,  C07D405/14 ,  C07D413/14

    摘要： Compounds of formula (IA) or (IB) are inhibitors of CD80 and useful in immunomodulation therapy: wherein Ar represents an optionally substituted monocyclic or bicyclic aromatic or heteroaromatic group having from 5 to 10 ring atoms; R1 and R2 independently represent H, or C1-C6 alkyl; R3 represents H; F; Cl; Br; —NO2; —CN; C1-C6 alkyl optionally substituted by F or CI; or C1-C6 alkoxy optionally substituted by F; R4 represents a carboxylic acid group (—COOH) or an ester thereof, or —C(═O)NR6R7, —NR7C(═O)R6, —NHC(═O)NR7R6 or —NHC(═S)NR7R6 wherein R6 represents H, or a radical of formula -(Alk)m-Q wherein m is 0 or 1, Alk is an optionally substituted divalent straight or branched C1-C12 alkylene, or C2-C12 alkenylene, or C2-C12 alkynylene radical or a divalent C3-C12 carbocyclic radical, any of which radicals may be interrupted by one or more —O—, —S— or —N(R8)— radicals wherein R8 represents H or C1-C4 alkyl, C3-C4 alkenyl, C3-C4 alkynyl, or C3-C6 cycloalkyl, and Q represents H; —CF3;—OH; —SH; —NR8R8 wherein each R8 may be the same or different, or form a ring when taken together with the nitrogen to which they are attached; an ester group; or an optionally substituted aryl, aryloxy, cycloalkyl, cycloalkenyl or heterocyclic group; and R7 represents H or C1-C6 alkyl; or when taken together with the atom or atoms to which they are attached R6 and R7 form a monocyclic heterocyclic ring having 5, 6 or 7 ring atoms; and X represents a bond or a divalent radical of formula —(Z)n-(Alk)- or -(Alk)-(Z)n— wherein Z represents -0-, —S— or —NH—, Alk is as defined in relation to R6 and n is 0 or 1.

    摘要翻译： 式（IA）或（IB）的化合物是CD80的抑制剂，可用于免疫调节治疗：其中Ar表示任选取代的具有5至10个环原子的单环或双环芳族或杂芳族基团; R1和R2独立地表示H或C1-C6烷基; R3表示H; F; Cl; Br; -NO2; -CN; 任选被F或Cl取代的C 1 -C 6烷基; 或任选被F取代的C 1 -C 6烷氧基; R 4表示羧酸基（-COOH）或其酯，或-C（= O）NR 6 R 7，-NR 7 C（= O）R 6，-NHC（= O）NR 7 R 6或-NHC（= H或其中m为0或1的式 - （Alk）mQ的基团，Alk为任选取代的二价直链或支链C 1 -C 12亚烷基或C 2 -C 12亚烯基或C 2 -C 12亚炔基或二价C 3- C12碳环基团，其中任何基团可以被一个或多个-O - ， - S-或-N（R 8） - 基团中断，其中R 8表示H或C 1 -C 4烷基，C 3 -C 4烯基，C 3 -C 4炔基， 或C 3 -C 6环烷基，Q表示H; -CF 3; -OH; -SH; -NR 8 R 8，其中每个R 8可以相同或不同，或者当与它们连接的氮一起取代时形成环; 酯基; 或任选取代的芳基，芳氧基，环烷基，环烯基或杂环基; 并且R 7表示H或C 1 -C 6烷基; 或者当与它们所连接的原子或原子一起时，R6和R7形成具有5,6或7个环原子的单环杂环; 并且X表示式 - （Z）n-（Alk） - 或 - （Alk） - （Z）n-的键或二价基团，其中Z表示-O - ， - S-或-NH-，Alk为 关于R6定义，n为0或1。

    Immunomodulating heterocyclic compounds
    7.
    发明授权
    Immunomodulating heterocyclic compounds 有权

    公开(公告)号：US07276505B2

    公开(公告)日：2007-10-02

    申请号：US10547448

    申请日：2004-03-10

    申请人： Ian Richard Matthews

    发明人： Ian Richard Matthews

    IPC分类号： A01N43/58 ,  A01N43/60 ,  A61K31/50 ,  A61K31/495 ,  C07D237/26 ,  C07D237/36 ,  C07D487/00

    CPC分类号： C07D487/04 ,  C07D519/00

    摘要： Compounds of formula (I) are inhibitors of CD80 and useful in immunomodulation therapy: wherein R1 and R3 independently represent H; F; CI; Br; —NO2; —CN; C1-C6 alkyl optionally substituted by F or Cl; or C1-C6 alkoxy optionally substituted by F; R4 represents a carboxylic acid group (—COOH) or an ester thereof, or —C(═O)NR6R7, —NR7C(═O)R6, —NR7C(═O)OR6, —NHC(═O)NR7R6 or —NHC(═S)NR7R6 wherein R6 represents H, or a radical of formula -(Alk)m-Q wherein m is 0 or 1, Alk is an optionally substituted divalent straight or branched C1-C12 alkylene, or C2-C12 alkenylene, or C2-C12 alkynylene radical or a divalent C3-C12 carbocyclic radical, any of which radicals may contain one or more —O—, —S— or —N(R8)— links wherein R8, represents H or C1-C4 alkyl, C3-C4 alkenyl, C3-C4 alkynyl, or C3-C6 cycloalkyl, and Q represents H; —NR9R10 wherein R9 and R10 independently represents H; C1-C4 alkyl; C3-C4 alkenyl; C3-C4 alkynyl; C3-C6 cycloalkyl; an ester group; an optionally substituted carbocyclic or heterocyclic group; or R9 and R10 form a ring when taken together with the nitrogen to which they are attached, which ring is optionally substituted; and R7 represents H or C1-C6 alkyl; or when taken together with the atom or atoms to which they are attached R6 and R7 form an optionally substituted monocyclic heterocyclic ring having 5, 6 or 7 ring atoms; and X represents a bond or a divalent radical of formula -(Z)n-(Alk)- or -(Alk)-(Z)n-wherein Z represents —O—, —S— or —NH—, Alk is as defined in relation to R6, and n is 0 or 1

    Immunomodulating Heterocyclic Compounds
    10.
    发明申请
    Immunomodulating Heterocyclic Compounds 有权
    免疫调节杂环化合物

    公开(公告)号：US20090312334A1

    公开(公告)日：2009-12-17

    申请号：US12545902

    申请日：2009-08-24

    申请人： Ian Richard Matthews

    发明人： Ian Richard Matthews

    IPC分类号： A61K31/5025 ,  C07D487/04

    CPC分类号： C07D487/04 ,  C07D519/00

    摘要： Compounds of formula (I) are inhibitors of CD80 and useful in immunomodulation therapy: wherein R1 and R3 independently represent H; F; Cl; Br; —NO2; —CN; C1-C6 alkyl optionally substituted by F or Cl; or C1-C6 alkoxy optionally substituted by F; R4 represents a carboxylic acid group (—COOH) or an ester thereof, or —C(═O)NR6R7, —NR7C(═O)R6, —NR7C(═O)OR6, —NHC(═O)NR7R6 or —NHC(═S)NR7R6 wherein R6 represents H, or a radical of formula -(Alk)m-Q wherein m is 0 or 1, Alk is an optionally substituted divalent straight or branched C1-C12 alkylene, or C2-C12 alkenylene, or C2-C12 alkynylene radical or a divalent C3-C12 carbocyclic radical, any of which radicals may contain one or more —O—, —S— or —N(R8)— links wherein R8 represents H or C1-C4 alkyl, C3-C4 alkenyl, C3-C4 alkynyl, or C3-C6 cycloalkyl, and Q represents H; —NR9R10 wherein R9 and R10 independently represents H; C1-C4 alkyl; C3-C4 alkenyl; C3-C4 alkynyl; C3-C6 cycloalkyl; an ester group; an optionally substituted carbocyclic or heterocyclic group; or R9 and R10 form a ring when taken together with the nitrogen to which they are attached, which ring is optionally substituted; and R7 represents H or C1-C6 alkyl; or when taken together with the atom or atoms to which they are attached R6 and R7 form an optionally substituted monocyclic heterocyclic ring having 5, 6 or 7 ring atoms; and X represents a bond or a divalent radical of formula -(Z)n-(Alk)- or -(Alk)-(Z)n- wherein Z represents —O—, —S— or —NH—, Alk is as defined in relation to R6 and n is 0 or 1.

    摘要翻译： 式（I）化合物是CD80的抑制剂，可用于免疫调节治疗：其中R1和R3独立地表示H; F; Cl; Br; -NO2; -CN; 任选被F或Cl取代的C 1 -C 6烷基; 或任选被F取代的C 1 -C 6烷氧基; R 4表示羧酸基（-COOH）或其酯，或-C（-O）NR 6 R 7，-NR 7 C（-O）R 6，-NR 7 C（-O）OR 6，-NHC（-O）NR 7 R 6或-NHC （-S）NR 7 R 6，其中R 6表示H，或式 - （Alk）m Q基团，其中m为0或1，Alk为任选取代的二价直链或支链C 1 -C 12亚烷基或C 2 -C 12亚链烯基， C 12亚炔基或二价C 3 -C 12碳环基团，其中任何基团可以含有一个或多个-O - ， - S-或-N（R 8） - 键，其中R 8表示H或C 1 -C 4烷基，C 3 -C 4链烯基 ，C 3 -C 4炔基或C 3 -C 6环烷基，Q表示H; -NR 9 R 10，其中R 9和R 10独立地表示H; C 1 -C 4烷基; C3-C4烯基; C3-C4炔基; C3-C6环烷基; 酯基; 任选取代的碳环或杂环基; 当与它们所连接的氮一起取代时，R 9和R 10形成环，该环任选被取代; 并且R 7表示H或C 1 -C 6烷基; 或者当与它们所连接的原子或原子一起时R6和R7形成任选取代的具有5,6或7个环原子的单环杂环; 并且X表示式 - （Z）n-（Alk） - 或 - （Alk） - （Z）n-的键或二价基团，其中Z表示-O - ， - S-或-NH-，Alk为 关于R6定义，n为0或1。