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    Compounds having CRTH2 antagonist activity
    1.
    发明授权
    Compounds having CRTH2 antagonist activity 有权
    具有CRTH2拮抗活性的化合物

    公开(公告)号：US08563536B2

    公开(公告)日：2013-10-22

    申请号：US13017860

    申请日：2011-01-31

    申请人： Richard Edward Armer ,  Eric Roy Pettipher ,  Mark Whittaker ,  Graham Michael Wynne ,  Julia Vile ,  Frank Schroer

    发明人： Richard Edward Armer ,  Eric Roy Pettipher ,  Mark Whittaker ,  Graham Michael Wynne ,  Julia Vile ,  Frank Schroer

    IPC分类号： A61K31/70 ,  A61K31/56 ,  A61K31/50 ,  A61K31/47 ,  A61K31/44

    CPC分类号： A61K31/4439 ,  A61K31/47 ,  A61K45/06 ,  C07D401/06

    摘要： Compounds of general formula (II) wherein W is chloro or fluoro; R1 is phenyl optionally substituted with one or more substituents, selected from halo, —CN, —C1-C6 alkyl, —SOR3, —SO2R3, —SO2N(R2)2, —N(R2)2, —NR2C(O)R3, —CO2R2, —CONR2R3, —NO2, —OR2, —SR2, —O(CH2)pOR2, or —O(CH2)pO(CH2)qOR2 wherein each R2 is independently hydrogen, —C1-C6 alkyl, —C3-C8 cycloalkyl, aryl or heteroaryl; each R3 is independently, —C1-C6 alkyl, —C3-C8 cycloalkyl, aryl or heteroaryl; p and q are each independently an integer from 1 to 3; and R4 is hydrogen, C1-C6 alkyl, C1-C6 alkyl substituted with aryl, aryl, (CH2)mOC(═O)C1-C6alkyl, ((CH2)mO)nCH2CH2X, (CH2)mN(R5)2 or CH((CH2)mO(C═O)R6)2; m is 1 or 2; n is 1-4; X is OR5 or N(R5)2; R5 is hydrogen or methyl; and R6 is C1-C18 alkyl; and their pharmaceutically acceptable salts, hydrates, solvates, complexes or prodrugs are useful in orally administrable compositions for the treatment of allergic diseases such as asthma, allergic rhinitis and atopic dermatitis.

    摘要翻译： 通式（II）的化合物，其中W是氯或氟; R 1是任选被一个或多个选自卤素，-CN，-C 1 -C 6烷基，-SOR 3，-SO 2 R 3，-SO 2 N（R 2）2，-N（R 2）2，-NR 2 C（O）R 3 ，-CO 2 R 2，-CONR 2 R 3，-NO 2，-OR 2，-SR 2，-O（CH 2）pOR 2或-O（CH 2）p O（CH 2）q OR 2，其中每个R 2独立地是氢，-C 1 -C 6烷基， C8环烷基，芳基或杂芳基; 每个R 3独立地是-C 1 -C 6烷基，-C 3 -C 8环烷基，芳基或杂芳基; p和q各自独立地为1至3的整数; 芳基，（CH2）mOC（= O）C1-C6烷基，（（CH2）mO）nCH2CH2X，（CH2）mN（R5）2或CH （（CH 2）m O（C = O）R 6）2; m为1或2; n为1-4; X为OR 5或N（R 5）2; R5是氢或甲基; R6为C1-C18烷基; 其药学上可接受的盐，水合物，溶剂合物，复合物或前药可用于口服给药的组合物中，用于治疗过敏性疾病如哮喘，过敏性鼻炎和特应性皮炎。

    Compounds having CRTH2 antagonist activity
    2.
    发明授权
    Compounds having CRTH2 antagonist activity 有权
    具有CRTH2拮抗活性的化合物

    公开(公告)号：US08536158B2

    公开(公告)日：2013-09-17

    申请号：US13014314

    申请日：2011-01-26

    申请人： Richard Edward Armer ,  Eric Roy Pettipher ,  Mark Whittaker ,  Graham Michael Wynne ,  Julia Vile ,  Frank Schroer

    发明人： Richard Edward Armer ,  Eric Roy Pettipher ,  Mark Whittaker ,  Graham Michael Wynne ,  Julia Vile ,  Frank Schroer

    IPC分类号： A61K31/70 ,  A61K31/56 ,  A61K31/50 ,  A61K31/47 ,  A61K31/44

    CPC分类号： A61K31/4439 ,  A61K31/47 ,  A61K45/06 ,  C07D401/06

    摘要： Compounds of general formula (I) wherein W is chloro or fluoro; R1 is phenyl optionally substituted with one or more substituents, selected from halo, —CN, —C1-C6 alkyl, —SOR3, —SO2R3, —SO2N(R2)2, —N(R2)2, —NR2C(O)R3, —CO2R2, —CONR2R3, —NO2, —OR2, —SR2, —O(CH2)pOR2, or —O(CH2)pO(CH2)qOR2 wherein each R2 is independently hydrogen, —C1-C6 alkyl, —C3-C8 cycloalkyl, aryl or heteroaryl; each R3 is independently, —C1-C6 alkyl, —C3-C8 cycloalkyl, aryl or heteroaryl; p and q are each independently an integer from 1 to 3; and R4 is hydrogen, C1-C6 alkyl, C1-C6 alkyl substituted with aryl, aryl, (CH2)mOC(═O)C1-C6alkyl, ((CH2)mO)nCH2CH2X, (CH2)mN(R5)2 or CH((CH2)mO(C═O)R6)2; m is 1 or 2; n is 1-4; X is OR5 or N(R5)2; R5 is hydrogen or methyl; and R6 is C1-C18 alkyl; and their pharmaceutically acceptable salts, hydrates, solvates, complexes or prodrugs are useful in orally administrable compositions for the treatment of allergic diseases such as asthma, allergic rhinitis and atopic dermatitis.

    摘要翻译： 通式（I）的化合物，其中W是氯或氟; R 1是任选被一个或多个选自卤素，-CN，-C 1 -C 6烷基，-SOR 3，-SO 2 R 3，-SO 2 N（R 2）2，-N（R 2）2，-NR 2 C（O）R 3 ，-CO 2 R 2，-CONR 2 R 3，-NO 2，-OR 2，-SR 2，-O（CH 2）pOR 2或-O（CH 2）p O（CH 2）q OR 2，其中每个R 2独立地是氢，-C 1 -C 6烷基， C8环烷基，芳基或杂芳基; 每个R 3独立地是-C 1 -C 6烷基，-C 3 -C 8环烷基，芳基或杂芳基; p和q各自独立地为1至3的整数; 芳基，（CH2）mOC（= O）C1-C6烷基，（（CH2）mO）nCH2CH2X，（CH2）mN（R5）2或CH （（CH 2）m O（C = O）R 6）2; m为1或2; n为1-4; X为OR 5或N（R 5）2; R5是氢或甲基; R6为C1-C18烷基; 其药学上可接受的盐，水合物，溶剂合物，复合物或前药可用于口服给药的组合物中，用于治疗过敏性疾病如哮喘，过敏性鼻炎和特应性皮炎。

    Compounds Having CRTH2 Antagonist Activity
    4.
    发明申请
    Compounds Having CRTH2 Antagonist Activity 有权
    具有CRTH2拮抗作用的化合物

    公开(公告)号：US20100063103A1

    公开(公告)日：2010-03-11

    申请号：US12625497

    申请日：2009-11-24

    申请人： Richard Edward ARMER ,  Eric Roy Pettipher ,  Mark Whittaker ,  Graham Michael Wynne ,  Julia Vile ,  Frank Schroer

    发明人： Richard Edward ARMER ,  Eric Roy Pettipher ,  Mark Whittaker ,  Graham Michael Wynne ,  Julia Vile ,  Frank Schroer

    IPC分类号： A61K31/4439 ,  C07D401/06 ,  A61P37/08

    CPC分类号： A61K31/4439 ,  A61K31/47 ,  A61K45/06 ,  C07D401/06

    摘要： Compounds of general formula (I) wherein W is chloro or fluoro; R1 is phenyl optionally substituted with one or more substituents, selected from halo, —CN, —C1-C6 alkyl, —SOR3, —SO2R3, —SO2N(R2)2, —N(R2)2, —NR2C(O)R3, —CO2R2, —CONR2R3, —NO2, —OR2, —SR2, —O(CH2)pOR2, or —O(CH2)pO(CH2)qOR2 wherein each R2 is independently hydrogen, —C1-C6 alkyl, —C3-C8 cycloalkyl, aryl or heteroaryl; each R3 is independently, —C1-C6 alkyl, —C3-C8 cycloalkyl, aryl or heteroaryl; p and q are each independently an integer from 1 to 3; and R4 is hydrogen, C1-C6 alkyl, C1-C6 alkyl substituted with aryl, aryl, (CH2)mOC(═O)C1-C6alkyl, ((CH2)mO)nCH2CH2X, (CH2)mN(R5)2 or CH((CH2)mO(C═O)R6)2; m is 1 or 2; n is 1-4; X is OR5 or N(R5)2; R5 is hydrogen or methyl; and R6 is C1-C18 alkyl; and their pharmaceutically acceptable salts, hydrates, solvates, complexes or prodrugs are useful in orally administrable compositions for the treatment of allergic diseases such as asthma, allergic rhinitis and atopic dermatitis.

    摘要翻译： 通式（I）的化合物，其中W是氯或氟; R 1是任选被一个或多个选自卤素，-CN，-C 1 -C 6烷基，-SOR 3，-SO 2 R 3，-SO 2 N（R 2）2，-N（R 2）2，-NR 2 C（O）R 3 ，-CO 2 R 2，-CONR 2 R 3，-NO 2，-OR 2，-SR 2，-O（CH 2）pOR 2或-O（CH 2）p O（CH 2）q OR 2，其中每个R 2独立地是氢，-C 1 -C 6烷基， C8环烷基，芳基或杂芳基; 每个R 3独立地是-C 1 -C 6烷基，-C 3 -C 8环烷基，芳基或杂芳基; p和q各自独立地为1至3的整数; 芳基，（CH2）mOC（= O）C1-C6烷基，（（CH2）mO）nCH2CH2X，（CH2）mN（R5）2或CH （（CH 2）m O（C = O）R 6）2; m为1或2; n为1-4; X为OR 5或N（R 5）2; R5是氢或甲基; R6为C1-C18烷基; 其药学上可接受的盐，水合物，溶剂合物，复合物或前药可用于口服给药的组合物中，用于治疗过敏性疾病如哮喘，过敏性鼻炎和特应性皮炎。

    Glyoxalase inhibitors
    5.
    发明申请
    Glyoxalase inhibitors 审中-公开
    乙二醛酶抑制剂

    公开(公告)号：US20070015799A1

    公开(公告)日：2007-01-18

    申请号：US10556901

    申请日：2004-05-14

    申请人： Mark Ashton ,  Alan Davidson ,  Russell Thomas ,  Mark Whittaker

    发明人： Mark Ashton ,  Alan Davidson ,  Russell Thomas ,  Mark Whittaker

    IPC分类号： A61K31/4436 ,  A61K31/44 ,  A61K31/381

    CPC分类号： C07D405/04 ,  A61K31/10 ,  A61K31/381 ,  A61K31/44 ,  A61K31/4436 ,  C07C323/62 ,  C07D213/85 ,  C07D217/26 ,  C07D409/04 ,  C07D409/14

    摘要： This invention relates to compounds of formula (I) which are glyoxalase I inhibitors, pharmaceutical salts or compositions comprising such compounds, and the use of such compositions and compounds to treat various conditions alleviated by the inhibition of glyoxalase 1. Wherein X is N or CH. R2 is H, CF3; or optionally substituted C5-6 aryl, C3-7 cycloalkyl, C5-7 heterocyclyl. R3 is H; or optionally substituted C5-6 aryl, C3-7 cycloalkyl, C5-7 heterocyclyl. Alternatively R2 and R3 together form an optionally substituted C3-4alkylene group wherein L3 and L4 are single bonds thus forming a C5-6 ring fused with the aromatic ring to which L3 and L4 are attached. L3 and L4 are independently selected from a single bond, optionally substituted C1-4 alkylene, -L9YN(OH)C(═O)L10- and -L9C(═O)N(OH)YL10-, wherein L9 and L10 are independently selected from optionally substituted C1-4 alkylene, C5-6 arylene, C1-4 alkylene-C5-6arylene and a single bond, wherein Y is NH or a single bond.

    摘要翻译： 本发明涉及作为乙二醛酶I抑制剂的式（I）化合物，包含这些化合物的药物盐或组合物，以及这些组合物和化合物用于治疗通过抑制乙二醛酶1减轻的各种病症的用途。其中X是N或CH 。 R 2是H，CF 3 N; 或任选取代的C 5-6芳基，C 3-7环烷基，C 5-7杂环基。 R 3是H; 或任选取代的C 5-6芳基，C 3-7环烷基，C 5-7杂环基。 或者R 2和R 3一起形成任选取代的C 3-4亚烷基，其中L 3和L 3 因此形成与L 3和L 4的芳环稠合的C 5〜6环， SUP>连接。 L 3和L 4独立地选自单键，任选取代的C 1-4亚烷基，-L 9， SUP-YN（OH）C（-O）L 10 - 和-L 9 C（ - ）N（OH）Y L 10 - ，其中L 9和L 10独立地选自任选取代的C 1-4 - 亚烷基，C 5-6 - 亚芳基，C 1-4亚烷基-C 5-6亚芳基和单键，其中Y是NH或单键。

    N-formyl hydroxylamine derivatives as antibacterial agents
    9.
    发明授权
    N-formyl hydroxylamine derivatives as antibacterial agents 失效
    N-甲酰羟胺衍生物作为抗菌剂

    公开(公告)号：US06476067B1

    公开(公告)日：2002-11-05

    申请号：US09868076

    申请日：2001-06-14

    申请人： Michael George Hunter ,  Raymond Paul Beckett ,  Martin John Clements ,  Mark Whittaker

    发明人： Michael George Hunter ,  Raymond Paul Beckett ,  Martin John Clements ,  Mark Whittaker

    IPC分类号： A61K3127

    CPC分类号： A61K31/351 ,  A61K31/223 ,  A61K31/445

    摘要： Compounds of formula (I) are in the preparation of antibacterial agents, wherein: R1 represents hydrogen, C1-C6 alkyl or C1-C6 alkyl substituted by one or more halogen atoms; R2 represents a group R10(X)n—(ALK)— wherein R10 represents hydrogen, a C1-C6 alkyl, C2-C6 alkenyl, C1-C6 alkynyl, cycloalkyl, aryl, or heterocyclyl group, any of which may be unsubstituted or substituted by (C1-C6)alkyl, (C1-C6)alkoyy, hydroxy, mercapto, (C1-C6)alkylthio, amino, halo, trifluoromethyl, cyano, nitro, —COOH, —CONH2, —COORA, —NHCORA, —CONHRA, —NHRA, —NRARB, or —CONRARB wherein RA and RB are independently a (C1-C6)alkyl group, and ALK represents a straight or branched divalent C1-C6 alkylene, C2-C6 alkenylene, or C2-C6 alkynylene radical, which may be interrupted by one or more non-adjacent —NH—, —O— or —S— linkages, X represents —NH—, —O— or —S—, and n is 0 or 1, R represents hydrogen or C1-C6 alkyl, R3 represents the characterising group or a natural or non-natural &agr; amino acid in which any functional groups may be protected; and R4 represents an ester or thioester group.

    摘要翻译： 式（I）化合物在制备抗菌剂中，其中：R1代表氢，C1-C6烷基或被一个或多个卤素原子取代的C1-C6烷基; R 2表示基团R 10（X）n-（ALK） - 其中R 10表示氢，C 1 -C 6烷基，C 2 -C 6烯基，C 1 -C 6炔基，环烷基，芳基或杂环基，其中任何一个可以是未取代的或 被（C 1 -C 6）烷基，（C 1 -C 6）烷基，羟基，巯基，（C 1 -C 6）烷硫基，氨基，卤素，三氟甲基，氰基，硝基，-COOH，-CONH 2，-COORA，-NHCORA - CONHRA，-NHRA，-NRARB或-CONRARB，其中RA和RB独立地为（C1-C6）烷基，ALK表示直链或支链二价C1-C6亚烷基，C2-C6亚烯基或C2-C6亚炔基 ，其可以被一个或多个不相邻的-NH-，-O-或-S-键中断，X表示-NH-，-O-或-S-，n为0或1，R表示氢或 C 1 -C 6烷基，R 3表示其中任何官能团可被保护的表征基团或天然或非天然α氨基酸; 并且R 4表示酯或硫酯基。