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    COMPOUNDS AS MODULATORS OF ENDOPLASMIC RETICULUM AMINOPEPTIDASE 1 (ERAP1)
    4.
    发明公开
    COMPOUNDS AS MODULATORS OF ENDOPLASMIC RETICULUM AMINOPEPTIDASE 1 (ERAP1) 审中-公开

    公开(公告)号：US20240300976A1

    公开(公告)日：2024-09-12

    申请号：US18004386

    申请日：2021-09-21

    Applicant: GREY WOLF THERAPEUTICS LIMITED

    Inventor： Martin QUIBELL ,  Jason John SHIERS ,  Michael SPARENBERG ,  Eleanor IVENS

    IPC: C07D515/04 ,  A61K31/4365 ,  A61K45/06

    CPC classification number: C07D515/04 ,  A61K31/4365 ,  A61K45/06

    Abstract: A compound of formula (I-1), or a pharmaceutically accept able salt or hydrate thereof, formula (I-1) wherein: ring A is a monocyclic 5, 6, or 7-membered heterocycloalkyl ring optionally substituted by one or more substituents selected from alkyl, CN, cycloalkyl, OH, alkoxy, halo, haloalkyl and heteroaryl, wherein said heteroaryl group is in turn optionally further substituted with one or more groups selected from halo and alkyl, and wherein one or two carbons in the 5, 6, or 7-membered heterocycloalkyl ring are optionally replaced by a group selected from O, NH, S and CO; L is a linker group which is a 2 to 7-membered saturated or unsaturated aliphatic group, wherein one or two carbon atoms in said group, other than the carbon atom directly bonded to ring A, are optionally replaced by a heteroatom-containing group selected from O, NH and S, and wherein when two carbon atoms are replaced, the heteroatom-containing groups are separated by at least two carbon atoms and the linker group is at least a 5-membered group; the group X—Y is —NR23SO2— or —SO2NR23—; R1 is H, CN or alkyl; R2 is selected from COOH, tetrazolyl and C(O)NHSO2R24; R3 is selected from H, halo and alkyl; R4 is selected from H and halo; R6 is H; R7 is selected from H, CN, haloalkyl, halo, SO2-alkyl, SO2NR18R19, CONR20R21, heteroaryl and alkyl, wherein said heteroaryl group is optionally substituted by one or more substituents select ed from alkyl, halo, alkoxy, CN, haloalkyl and OH; R8 is selected from H, alkyl, haloalkyl and halo; R9 is H, alkyl or halo; R18-R21 and R23 are each independently selected from H and alkyl; R24 is selected from alkyl and cyclopropyl. Further aspects of the invention relate to such compounds for use in the field of immuno-oncology and related applications.

    COMPOUNDS
    5.
    发明申请
    COMPOUNDS 有权

    公开(公告)号：US20230064417A1

    公开(公告)日：2023-03-02

    申请号：US17295335

    申请日：2019-11-22

    Applicant: GREY WOLF THERAPEUTICS LIMITED

    Inventor： Martin QUIBELL ,  Anil Lallubhai PATEL ,  Jason John SHIERS ,  Michael SPARENBERG ,  Peter Ian JOYCE

    IPC: A61K39/39 ,  A61K39/395 ,  C07D295/135 ,  C07D211/14 ,  C07D498/08 ,  C07D487/04 ,  C07D211/38 ,  C07D471/08 ,  C07D491/107 ,  C07D211/48 ,  C07D211/44 ,  C07D205/04 ,  C07D207/12 ,  C07D209/44 ,  A61K31/451 ,  A61K31/55 ,  A61K31/407 ,  A61K31/439 ,  A61K31/397 ,  A61K31/402 ,  A61K31/4035 ,  A61K31/553 ,  A61K31/495 ,  A61K31/438 ,  A61K31/4985 ,  A61K31/454 ,  A61K31/501 ,  A61K31/41 ,  A61K31/497

    Abstract: The present invention relates to a compound of formula (Ia), or a pharmaceutically acceptable salt or hydrate thereof, wherein: the group X-Y is —NHSO2— or —SO2NH—; R1 is H or alkyl; R2 is selected from COOH and a tetrazolyl group; R3 is selected from H, Cl and alkyl; R4 is selected from H, Cl and F; R5 is selected from H, alkyl, alkynyl, alkenyl, haloalkyl, SO2-alkyl, Cl, alkoxy, OH, CN, hydroxyalkyl, alkylthio, heteroaryl, cycloalkyl, heterocycloalkyl and haloalkoxy; R6 is H; R7 is selected from H, CN, haloalkyl, Cl, F, SO2-alkyl, SO2NR13R14, optionally substituted heteroaryl and alkyl; R8 is selected from H, alkyl, haloalkyl and halo; R9 is H, C1-C3-alkyl, or halo; R10 and R11, together with the nitrogen to which they are attached, form an azepanyl group, wherein (a) said azepanyl group is substituted by one or more substituents, or (b) one or two carbons in said azepanyl group are replaced by a group selected from O, NH, S and CO, and said azepanyl group is optionally further substituted; or R10 and R11, together with the nitrogen to which they are attached, form an azetidinyl, pyrrolidinyl or piperidinyl group wherein (a) said azetidinyl, pyrrolidinyl or piperidinyl group is substituted by one or more substituents, or (b) one or two carbons in said azetidinyl, pyrrolidinyl or piperidinyl group are replaced by a group selected from NH, S and CO; or R10 and R11, together with the nitrogen to which they are attached, form an 8, 9 or 10-membered bicyclic heterocycloalkyl group, wherein one or two carbons in the bicyclic heterocycloalkyl ring are optionally replaced by a group selected from O, NH, S and CO, and said bicyclic heterocycloalkyl group is optionally substituted; or R10 and R11, together with the nitrogen to which they are attached, form a 6 to 12-membered bicyclic group containing a spirocyclic carbon atom, wherein one or two carbons in the bicyclic group are optionally replaced by a group selected from O, NH, S and CO, and said bicyclic group is optionally substituted, or said bicyclic group is optionally fused to a 5 or 6-membered aryl or heteroaryl group; R13 and R14 are each independently H or alkyl. Further aspects of the invention relate to such compounds for use in the field of immune-oncology and related applications.

    ERAP1 MODULATORS
    6.
    发明申请
    ERAP1 MODULATORS 有权

    公开(公告)号：US20230000851A1

    公开(公告)日：2023-01-05

    申请号：US17774239

    申请日：2020-11-12

    Applicant: GREY WOLF THERAPEUTICS LIMITED

    Inventor： Martin QUIBELL ,  Michael SPARENBERG ,  Jason John SHIERS

    IPC: A61K31/451 ,  C07D211/28 ,  C07D257/04 ,  C07D207/09 ,  C07C311/21 ,  C07C317/34 ,  C07D211/34 ,  C07D401/10 ,  C07D417/10 ,  A61K31/41 ,  A61K31/40 ,  A61K31/196 ,  A61K31/277 ,  A61K31/454 ,  A61K35/15 ,  A61K39/00 ,  A61K39/395

    Abstract: The present invention relates to a compound of formula (I), or a pharmaceutically acceptable salt or hydrate thereof, A compound of formula (I), or a pharmaceutically acceptable salt or hydrate thereof, (I) wherein: Z is a group of formula: (II) wherein P and Q are each independently CR12R13; or one of P and Q is NR14 and the other is CR12R13; the group X—Y is —NHSO2— or —SO2NH—; R1 is H, CN or alkyl; R2 is selected from COOH and a tetrazolyl group; R3 is selected from H, Cl and alkyl; R4 is selected from H and halo; R5 is selected from H, alkyl, haloalkyl, SO2-alkyl, Cl, alkoxy, OH, CN, hydroxyalkyl, alkylthio, heteroaryl, cycloalkyl, heterocycloalkyl and haloalkoxy; R6 is H; R7 is selected from H, CN, haloalkyl, halo, SO2-alkyl, heteroaryl, SO2NR16R17, CONR10R11 and alkyl, wherein said heteroaryl group is optionally substituted by one or more substituents selected from alkyl, halo, alkoxy, CN, haloalkyl and OH; R8 is selected from H, alkyl, haloalkyl and halo; R9 is H or halo; and R10, R11, R12, R13, R14, R16 and R17 are each independently H or alkyl; R15 is selected from alkyl, halo, alkoxy, CN, haloalkyl and OH; and m and n are each independently 0, 1, 2 or 3. Further aspects of the invention relate to such compounds for use in the field of immune-oncology and related applications.

    PHENYL-SULFAMOYL-BENZOIC ACID DERIVATIVES AS ERAP1- MODULATORS
    7.
    发明申请
    PHENYL-SULFAMOYL-BENZOIC ACID DERIVATIVES AS ERAP1- MODULATORS 有权

    公开(公告)号：US20240376046A1

    公开(公告)日：2024-11-14

    申请号：US18291714

    申请日：2022-07-29

    Applicant: GREY WOLF THERAPEUTICS LIMITED

    Inventor： Martin QUIBELL ,  Jason John SHIERS ,  John FEUTRILL

    IPC: C07C311/21 ,  A61K31/196 ,  A61K31/275 ,  A61K31/337 ,  A61K31/341 ,  A61K31/397 ,  A61K31/41 ,  A61K31/42 ,  A61K31/425 ,  A61K45/06 ,  C07D205/04 ,  C07D257/04 ,  C07D261/08 ,  C07D275/02 ,  C07D305/06 ,  C07D305/14 ,  C07D307/12 ,  C07D309/12 ,  C07D493/08

    Abstract: The present invention relates to a compound of formula (I), or a pharmaceutically acceptable salt or hydrate thereof, Formula (I), wherein, the group X—Y is —NHSO2—; Z is a monocyclic or polycyclic cycloalkyl group or a monocyclic or polycyclic heterocycloalkyl group, each of which is optionally substituted by one or more groups selected from haloalkyl, alkyl, alkenyl, alkynyl and —(CR16R17)mR18, where m is 0 to 6; L is a direct bond or a group (CR14R15)n, where n is 1 or 2; R1 is H, CN, Cl or F or alkyl; R2 is selected from COOH and a tetrazolyl group; R3 is selected from H, halo, alkoxy and alkyl; R4 is selected from H and halo; R5 is selected from H, alkyl, haloalkyl, SO2-alkyl, Cl, alkoxy, OH, CN, hydroxyalkyl, alkylthio, heteroaryl, cycloalkyl, heterocycloalkyl and haloalkoxy; R6 is H; R7 is selected from H, CN, haloalkyl, halo, SO2-alkyl, SO2NR12R13, heteroaryl, CONR10R11 and alkyl, wherein said heteroaryl group is optionally substituted by one or more substituents selected from alkyl, halo, alkoxy, CN, haloalkyl and OH; R9 is selected from H, alkyl and halo; Rio, R1, R12 and R13 are each independently H or alkyl; R14 and R15 are each independently H, halo or alkyl; R16 and R17 are each independently H, halo, haloalkyl or alkyl; and each R18 is independently selected from OH, CN, alkoxy and halo. Further aspects of the invention relate to such compounds for use in the field of immune-oncology and related applications.

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