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    Substituted benzamidines as antibacterial agents
    5.
    发明授权
    Substituted benzamidines as antibacterial agents 有权

    公开(公告)号：US08415383B2

    公开(公告)日：2013-04-09

    申请号：US12679334

    申请日：2008-09-22

    申请人： David John Haydon ,  Ian Collins ,  Lloyd George Czaplewski

    发明人： David John Haydon ,  Ian Collins ,  Lloyd George Czaplewski

    IPC分类号： A01N43/40 ,  A61K31/44

    CPC分类号： C07D277/34 ,  A61K31/4245 ,  A61K31/427 ,  A61K31/429 ,  A61K31/433 ,  C07D271/07 ,  C07D277/64 ,  C07D285/08 ,  C07D417/12

    摘要： Compounds of formula (IA) or (IB) have antibacterial activity: wherein W is ═C(H)— or ═N—; R3 is a radical of formula -(Alk1)m-(Z1)p-(Alk2)n-Q wherein m, p and n are independently 0 or 1, provided that at least one of m, p and n is 1, Z1 is —O—, —S—, —S(O)—, —S(O2)—, —NH—, —N(CH3)—, —N(CH2CH3)—, —C(—O)—, —0—(C═O)—, —C(═O)—O—, or an optionally substituted divalent monocyclic carbocyclic or heterocyclic radical having 3 to 6 ring atoms; or an optionally substituted divalent bicyclic carbocyclic or heterocyclic radical having 5 to 10 ring atoms; Alk1 and Alk2 are optionally substituted C1-C6 alkylene, C2-C6 alkenylene, or C2-C6 alkynylene radicals, which may optionally terminate with or be interrupted by —O—, —S—, —S(O)—, —S(O2)—, —NH—, —N(CH3)—, Or —N(CH2CH3)—; and Q is hydrogen, halogen, nitrile, or hydroxyl, or an optionally substituted monocyclic carbocyclic or heterocyclic radical having 3 to 6 ring atoms; or an optionally substituted bicyclic carbocyclic or heterocyclic radical having 5 to 10 ring atoms; R4 and R5 are optional substituents; and R2, R6 and R7 are independently hydrogen or a radical of formula -(Alk3)x-(Z2)y-(Alk4)z-H wherein x, y and z are independently 0 or 1, Z2 is —O—, —S—, —S(O)—, —S(O2)—, —NH—, —N(CH3)—, —N(CH2CH3)—, —C(—O)—, —0—(C═O)— or —C(═O)—O—; Alk3 and Alk4 are optionally substituted C1-C3 alkylene, C2-C3 alkenylene, or C2-C3 alkynylene radicals, which may optionally terminate with or be interrupted by —O—, —S—, —S(O)—, —S(O2)—, —NH—, —N(CH3)—, or —N(CH2CH3)—.

    Antibacterial agents
    7.
    发明授权
    Antibacterial agents 有权
    抗菌剂

    公开(公告)号：US08492414B2

    公开(公告)日：2013-07-23

    申请号：US12678767

    申请日：2008-09-22

    申请人： David John Haydon ,  Ian Collins ,  Lloyd George Czaplewski

    发明人： David John Haydon ,  Ian Collins ,  Lloyd George Czaplewski

    IPC分类号： A61K31/41

    CPC分类号： C07D285/08

    摘要： Compounds of formula (IA) or (IB) have antibacterial activity: wherein W is ═CH— or ═N—; Ri and R2 are independently selected from hydrogen, fluoro and chloro, provided that Ri and R2 are not each hydrogen when W is ═CH—; n is 0 or 1; X is —O—, —S—, or —CH2—; and Q is (i) a phenyl radical, a naphthyl radical, a monocyclic carbocyclic or heteroaryl radical having 3 to 6 ring atoms, or a bicyclic heteroaryl radical having 5 to 10 ring atoms, any of which radicals being optionally substituted; or (ii) an optionally substituted C1-C6 alkyl, C2-C6 alkenyl, or C2-C6 alkynyl radical, which may optionally be interrupted by —O—, —S—, —S(O)—, —S(O2)—, —NH—, —N(CH3)—, —N(CH2CH3)—, —C—K═Oh or —C(═O)—O—.

    摘要翻译： 式（IA）或（IB）的化合物具有抗菌活性：其中W为= CH-或= N-; R 1和R 2独立地选自氢，氟和氯，条件是当W = CH-时，R 1和R 2不是氢。 n为0或1; X是-O - ， - S-或-CH 2 - ; Q为（i）具有3〜6个环原子的苯基，萘基，单环碳环或杂芳基，或环原子数为5〜10的双环杂芳基，其中任意一个为任选被取代的基团; 或（ⅱ）任选被-O - ， - S - ， - S（O） - ， - S（O 2））间隔的任选取代的C 1 -C 6烷基，C 2 -C 6烯基或C 2 -C 6炔基， - ， - NH - ， - N（CH 3） - ， - N（CH 2 CH 3） - ， - K = O或-C（= O）-O-。

    SUBSTITUTED BENAMIDINES AS ANTIBACTERIAL AGENTS
    8.
    发明申请
    SUBSTITUTED BENAMIDINES AS ANTIBACTERIAL AGENTS 有权

    公开(公告)号：US20100298388A1

    公开(公告)日：2010-11-25

    申请号：US12679334

    申请日：2008-09-22

    申请人： David John Haydon ,  Ian Collins ,  Lloyd George Czaplewski

    发明人： David John Haydon ,  Ian Collins ,  Lloyd George Czaplewski

    IPC分类号： A61K31/4245 ,  A61K31/433 ,  A61K31/428 ,  A61K31/427 ,  C07D285/08 ,  C07D413/12 ,  C07D277/64 ,  C07D413/04 ,  A01N43/78 ,  A01N43/836 ,  A01P1/00 ,  A61P31/04

    CPC分类号： C07D277/34 ,  A61K31/4245 ,  A61K31/427 ,  A61K31/429 ,  A61K31/433 ,  C07D271/07 ,  C07D277/64 ,  C07D285/08 ,  C07D417/12

    摘要： Compounds of formula (IA) or (IB) have antibacterial activity: wherein W is ═C(H)— or ═N—; R3 is a radical of formula -(Alk1)m-(Z1)p-(Alk2)n-Q wherein m, p and n are independently 0 or 1, provided that at least one of m, p and n is 1, Z1 is —O—, —S—, —S(O)—, —S(O2)—, —NH—, —N(CH3)—, —N(CH2CH3)—, —C(—O)—, —O—(C═O)—, —C(═O)—O—, or an optionally substituted divalent monocyclic carbocyclic or heterocyclic radical having 3 to 6 ring atoms; or an optionally substituted divalent bicyclic carbocyclic or heterocyclic radical having 5 to 10 ring atoms; Alk1 and Alk2 are optionally substituted C1-C6 alkylene, C2-C6 alkenylene, or C2-C6 alkynylene radicals, which may optionally terminate with or be interrupted by —O—, —S—, —S(O)—, —S(O2)—, —NH—, —N(CH3)—, Or —N(CH2CH3)—; and Q is hydrogen, halogen, nitrile, or hydroxyl, or an optionally substituted monocyclic carbocyclic or heterocyclic radical having 3 to 6 ring atoms; or an optionally substituted bicyclic carbocyclic or heterocyclic radical having 5 to 10 ring atoms; R4 and R5 are optional substituents; and R2, R6 and R7 are independently hydrogen or a radical of formula -(Alk3)x-(Z2)y-(Alk4)z-H wherein x, y and z are independently 0 or 1, Z2 is —O—, —S—, —S(O)—, —S(O2)—, —NH—, —N(CH3)—, —N(CH2CH3)—, —C(—O)—, —O—(C═O)— or —C(═O)—O—; Alk3 and Alk4 are optionally substituted C1-C3 alkylene, C2-C3 alkenylene, or C2-C3 alkynylene radicals, which may optionally terminate with or be interrupted by —O—, —S—, —S(O)—, —S(O2)—, —NH—, —N(CH3)—, or —N(CH2CH3)—.

    ANTIBACTERIAL AGENTS
    9.
    发明申请
    ANTIBACTERIAL AGENTS 有权
    抗菌剂

    公开(公告)号：US20100273837A1

    公开(公告)日：2010-10-28

    申请号：US12678767

    申请日：2008-09-22

    申请人： David John Haydon ,  Ian Collins ,  Lloyd George Czaplewski

    发明人： David John Haydon ,  Ian Collins ,  Lloyd George Czaplewski

    IPC分类号： A61K31/433 ,  C07D285/08 ,  A61P31/04 ,  A01N43/836 ,  A01P1/00

    CPC分类号： C07D285/08

    摘要： Compounds of formula (IA) or (IB) have antibacterial activity: wherein W is ═CH— or ═N—; Ri and R2 are independently selected from hydrogen, fluoro and chloro, provided that Ri and R2 are not each hydrogen when W is ═CH—; n is 0 or 1; X is —O—, —S—, or —CH2—; and Q is (i) a phenyl radical, a naphthyl radical, a monocyclic carbocyclic or heteroaryl radical having 3 to 6 ring atoms, or a bicyclic heteroaryl radical having 5 to 10 ring atoms, any of which radicals being optionally substituted; or (ii) an optionally substituted C1-C6 alkyl, C2-C6 alkenyl, or C2-C6 alkynyl radical, which may optionally be interrupted by —O—, —S—, —S(O)—, —S(O2)—, —NH—, —N(CH3)—, —N(CH2CH3)—, —C—K═Oh or —C(═O)—O—.

    摘要翻译： 式（IA）或（IB）的化合物具有抗菌活性：其中W是= CH-或= N-; R 1和R 2独立地选自氢，氟和氯，条件是当W是= CH-时，R 1和R 2不是氢。 n为0或1; X是-O - ， - S-或-CH 2 - ; Q为（i）具有3〜6个环原子的苯基，萘基，单环碳环或杂芳基，或环原子数为5〜10的双环杂芳基，其中任意一个为任选被取代的基团; 或（ⅱ）任选被-O - ， - S - ， - S（O） - ， - S（O 2））间隔的任选取代的C 1 -C 6烷基，C 2 -C 6烯基或C 2 -C 6炔基， - ， - NH - ， - N（CH 3） - ， - N（CH 2 CH 3） - ， - C-K = Oh或-C（= O）-O-。

    Purine and deazapurine derivatives as pharmaceutical compounds
    10.
    发明授权
    Purine and deazapurine derivatives as pharmaceutical compounds 有权

    公开(公告)号：US08796293B2

    公开(公告)日：2014-08-05

    申请号：US12298462

    申请日：2007-04-25

    申请人： Thomas Glanmor Davies ,  Michelle Dawn Garrett ,  Robert George Boyle ,  Ian Collins

    发明人： Thomas Glanmor Davies ,  Michelle Dawn Garrett ,  Robert George Boyle ,  Ian Collins

    IPC分类号： A61K31/519 ,  A61K31/44 ,  C07D471/04 ,  C07D473/34

    CPC分类号： C07D471/04 ,  C07D473/34 ,  C07D487/04

    摘要： The invention provides a compound of the formula (I) or salts, solvates, tautomers or N-oxides thereof, wherein T is N or CR5; J1-J2 is N═C(R6), (R7)C═N, (R8)N—C(O), (R8)2C—C(O), N═N or (R7)C═C(R6); E is a monocyclic carbocyclic or heterocyclic group of 5 or 6 ring members, the heterocyclic group containing up to 3 heteroatoms selected from O, N and S; Q1 is a bond or a saturated C1-3 hydrocarbon linker group, one of the carbon atoms in the linker group being optionally be replaced by an oxygen or nitrogen atom, or an adjacent pair of carbon atoms may be replaced by CONRq or NRqCO where Rq is hydrogen or methyl, or Rq is a C1-4alkylene chain linked to R1 or a carbon atom of Q1 to form a cyclic moiety; and wherein the carbon atoms of the linker group Q1 may optionally bear one or more substituents selected from fluorine and hydroxy; Q2 is a bond or a saturated hydrocarbon linker group containing from 1 to 3 carbon atoms, wherein one of the carbon atoms in the linker group may optionally be replaced by an oxygen or nitrogen atom; and wherein the carbon atoms of the linker group may optionally bear one or more substituents selected from fluorine and hydroxy, provided that the hydroxy group when present is not located at a carbon atom α with respect to the G group; and provided that when E is aryl or heteroaryl, then Q2 is other than a bond; G is hydrogen, NR2R3, OH or SH provided that when E is aryl or heteroaryl and Q2 is a bond, then G is hydrogen; R1 is hydrogen or an aryl or heteroaryl group, with the proviso that when R1 is hydrogen and G is NR2R3, then Q2 is a bond; and R2, R3R4, R6 and R8 are as defined in the claims, wherein the compound is for use in: (a) the treatment or prophylaxis of a disease or condition in which the modulation (e.g. inhibition) of ROCK kinase or protein kinase P70S6K is indicated; and/or (b) the treatment of a subject or patient population in which the modulation (e.g. inhibition) of ROCK kinase or protein kinase P70S6K is indicated.