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    Potassium ion channel modulators and uses thereof
    1.
    发明授权
    Potassium ion channel modulators and uses thereof 有权

    公开(公告)号：US09464052B2

    公开(公告)日：2016-10-11

    申请号：US13054960

    申请日：2009-07-20

    申请人： Simon David Edwards ,  Meriel Ruth Kimberley ,  Richard Edward Armer ,  Nawaz Mohammed Khan

    发明人： Simon David Edwards ,  Meriel Ruth Kimberley ,  Richard Edward Armer ,  Nawaz Mohammed Khan

    IPC分类号： C07C237/20 ,  C07D213/40

    CPC分类号： A61K31/165 ,  A61K31/198 ,  A61K31/40 ,  A61K31/4402 ,  A61K31/445 ,  A61K31/5375 ,  A61K45/06 ,  C07C237/20 ,  C07D213/40

    摘要： Compounds of formula (I) and pharmacologically acceptable salts and pro-drugs thereof wherein: Ar1 and Ar2 are aryl or heteroaryl; a is 0 to 5; R1 is alkyl, halogen, haloalkyl, alkoxy, haloalkoxy, alkoxycarbonyl, carboxyl, hydroxyl, amino, monoalkylamino, dialkylamino, nitro, acylamino, alkoxycarbonylamino, alkylsulphonyl, alkylsulphonylamino or cyano and, where a is greater than 1, each substituent R1 may be the same or different; b is 0 to 5; R2 is alkyl, halogen, haloalkyl, haloalkoxy, alkoxy, alkoxycarbonyl, carboxyl, hydroxyl, amino, monoalkylamino, dialkylamino, nitro, acylamino, alkoxycarbonylamino, alkylsulphonyl, alkylsulphonylamino or cyano and where b is greater than 1, each substituent R2 may be the same or different; V is selected from the group consisting of (CR3aR3b)pCON(R3b)X and (CR3aR3b)pN(R3b)CO(X), wherein said groups are in the 3- (meta) or 4- (para) position with respect to the substituent Z; W is selected from the group consisting of NR4a, O, S, S═O, SO2 and C(R4aR4b)2; X is hydrogen, alkyl, hydroxyalkyl, alkoxyalkyl, haloalkoxyalkyl, aryloxyalkyl, cycloalkyl, aryl, heteroaryl, polyalkylene glycol, aminoalkyl, monoalkylaminoalkyl, dialkylaminoalkyl, alkyl that is substituted with a groups of formula of formula NR8R9 wherein R8 and R9 together with the nitrogen atom to which they are attached form a saturated or partially unsaturated heterocyclic group, carboxyalkyl, alkoxycarbonylalkyl, haloalkoxycarbonylalkyl or aralkyloxycarbonylalkyl; Y and Z are the same or different and each is a substituent selected from the group consisting of (CR5aR5b)n1, C═O, SO2, C(═O)NR5a; C(═O)NR5aSO2 and C═O(R5aR5b)n2; R3a, R3b, R4a, R4b, R5a and R5b are the same or different and each is selected from the hydrogen, alkyl, cycloalkyl, aryl and heteroaryl; n1 and n2 are the same or different and each is 0 to 2; and p is 0 to 2; are potassium ion channel modulators, making them particularly useful in treating and preventing conditions such as pain, lower urinary tract disorders and the like.

    Compounds Having CRTH2 Antagonist Activity
    2.
    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：US20090192195A1

    公开(公告)日：2009-07-30

    申请号：US12357821

    申请日：2009-01-22

    申请人： Richard Edward Armer ,  Carole Eliane Andree Maillol ,  Colin Richard Dorgan ,  Graham Michael Wynne ,  Julia Vile

    发明人： Richard Edward Armer ,  Carole Eliane Andree Maillol ,  Colin Richard Dorgan ,  Graham Michael Wynne ,  Julia Vile

    IPC分类号： A61K31/404 ,  C07D209/10 ,  C07D401/12 ,  A61K31/454 ,  A61P31/16 ,  A61P37/00

    CPC分类号： C07D209/10

    摘要： Compounds of general formula (I) wherein W is chloro or fluoro; Z is a group SO2R1; wherein R1 is —C3-C8 cycloalkyl or heterocyclyl optionally substituted with one or more substituents chosen 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, and —O(CH2)p—O—(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 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; Z是SO2R1基团; 其中R 1为-C 3 -C 8环烷基或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和-O（CH 2）p O-（CH 2）q OR 2，其中每个R 2独立地是氢， -C6烷基，-C3-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; 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。

    POTASSIUM ION CHANNEL MODULATORS & USES THEREOF
    4.
    发明申请
    POTASSIUM ION CHANNEL MODULATORS & USES THEREOF 有权

    公开(公告)号：US20110245250A1

    公开(公告)日：2011-10-06

    申请号：US13054960

    申请日：2009-07-20

    申请人： Simon David Edwards ,  Meriel Ruth Kimberley ,  Richard Edward Armer ,  Nawaz Mohammed Khan

    发明人： Simon David Edwards ,  Meriel Ruth Kimberley ,  Richard Edward Armer ,  Nawaz Mohammed Khan

    IPC分类号： A61K31/165 ,  C07C237/20 ,  A61K31/198 ,  C07D295/13 ,  A61K31/5375 ,  C07D207/12 ,  A61K31/40 ,  C07D211/06 ,  A61K31/445 ,  C07D213/40 ,  A61K31/4402 ,  A61P25/22 ,  A61P3/00 ,  A61P27/02 ,  A61P9/00 ,  A61P9/06 ,  A61P1/00

    CPC分类号： A61K31/165 ,  A61K31/198 ,  A61K31/40 ,  A61K31/4402 ,  A61K31/445 ,  A61K31/5375 ,  A61K45/06 ,  C07C237/20 ,  C07D213/40

    摘要： Compounds of formula (I) and pharmacologically acceptable salts and pro-drugs thereof wherein: Ar1 and Ar2 are aryl or heteroaryl; a is 0 to 5; R1 is alkyl, halogen, haloalkyl, alkoxy, haloalkoxy, alkoxycarbonyl, carboxyl, hydroxyl, amino, monoalkylamino, dialkylamino, nitro, acylamino, alkoxycarbonylamino, alkylsulphonyl, alkylsulphonylamino or cyano and, where a is greater than 1, each substituent R1 may be the same or different; b is 0 to 5; R2 is alkyl, halogen, haloalkyl, haloalkoxy, alkoxy, alkoxycarbonyl, carboxyl, hydroxyl, amino, monoalkylamino, dialkylamino, nitro, acylamino, alkoxycarbonylamino, alkylsulphonyl, alkylsulphonylamino or cyano and where b is greater than 1, each substituent R2 may be the same or different; V is selected from the group consisting of (CR3aR3b)pCON(R3b)X and (CR3aR3b)pN(R3b)CO(X), wherein said groups are in the 3- (meta) or 4- (para) position with respect to the substituent Z; W is selected from the group consisting of NR4a, O, S, S═O, SO2 and C(R4aR4b)2; X is hydrogen, alkyl, hydroxyalkyl, alkoxyalkyl, haloalkoxyalkyl, aryloxyalkyl, cycloalkyl, aryl, heteroaryl, polyalkylene glycol, aminoalkyl, monoalkylaminoalkyl, dialkylaminoalkyl, alkyl that is substituted with a groups of formula of formula NR8R9 wherein R8 and R9 together with the nitrogen atom to which they are attached form a saturated or partially unsaturated heterocyclic group, carboxyalkyl, alkoxycarbonylalkyl, haloalkoxycarbonylalkyl or aralkyloxycarbonylalkyl; Y and Z are the same or different and each is a substituent selected from the group consisting of (CR5aR5b)n1, C═O, SO2, C(═O)NR5a; C(═O)NR5aSO2 and C═O(R5aR5b)n2; R3a, R3b, R4a, R4b, R5a and R5b are the same or different and each is selected from the hydrogen, alkyl, cycloalkyl, aryl and heteroaryl; n1 and n2 are the same or different and each is 0 to 2; and p is 0 to 2; are potassium ion channel modulators, making them particularly useful in treating and preventing conditions such as pain, lower urinary tract disorders and the like.

    Compounds Having CRTH2 Antagonist Activity
    6.
    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：US20110123547A1

    公开(公告)日：2011-05-26

    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： A61K39/395 ,  A61K31/4439 ,  A61K31/522 ,  A61K31/573 ,  A61K31/519 ,  A61K31/58 ,  A61K33/24 ,  A61P31/12 ,  A61P11/00 ,  A61P1/00 ,  A61P31/16

    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
    7.
    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：US20100266535A1

    公开(公告)日：2010-10-21

    申请号：US12828800

    申请日：2010-07-01

    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： A61K38/20 ,  A61K31/4439 ,  A61K31/522 ,  A61K31/47 ,  A61K39/395 ,  A61K31/56 ,  A61K39/42 ,  A61P9/00 ,  A61P11/00 ,  A61P19/00 ,  A61P25/00 ,  A61P17/00 ,  A61P29/00 ,  A61P31/00 ,  A61P35/00 ,  A61P37/00

    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
    8.
    发明申请
    Compounds Having CRTH2 Antagonist Activity 审中-公开
    具有CRTH2拮抗作用的化合物

    公开(公告)号：US20090186923A1

    公开(公告)日：2009-07-23

    申请号：US12356822

    申请日：2009-01-21

    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

    CPC分类号： 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, and —O(CH2)p—O—(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 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） -COR 2 R 3，-NO 2，-OR 2，-SR 2，-O（CH 2）pOR 2和-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; 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。