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1. 发明申请

US20160367564A1 Pharmaceutical Compound 有权
公开(公告)号：US20160367564A1
公开(公告)日：2016-12-22
申请号：US15100494
申请日：2014-12-02
申请人： IOMET PHARMA LTD
发明人： Phillip Martin Cowley , Alan Wise , Margaret Huggett
IPC分类号： A61K31/551 , C07D401/04 , A61K31/454 , C07D401/14 , C07D471/04 , A61K31/4545 , A61K31/4439 , C07D413/14 , C07D409/14 , A61K31/444 , C07D405/14 , A61K31/4725 , C07D209/40 , A61K31/496 , A61K31/498 , C07D403/04 , A61K31/404 , C07D471/10 , A61K31/435 , C07D401/06 , C07D209/20 , C07D403/06 , A61K31/55 , A61K31/506 , C07D487/04 , A61K31/4985 , A61K31/5377 , A61K31/497 , C07D513/04 , A61K45/06
CPC分类号： A61K31/551 , A61K31/404 , A61K31/435 , A61K31/4439 , A61K31/444 , A61K31/454 , A61K31/4545 , A61K31/4725 , A61K31/496 , A61K31/497 , A61K31/498 , A61K31/4985 , A61K31/506 , A61K31/5377 , A61K31/55 , A61K45/06 , C07D209/20 , C07D209/34 , C07D209/40 , C07D401/04 , C07D401/06 , C07D401/12 , C07D401/14 , C07D403/04 , C07D403/06 , C07D403/12 , C07D405/12 , C07D405/14 , C07D409/14 , C07D413/12 , C07D413/14 , C07D471/04 , C07D471/10 , C07D487/04 , C07D513/04
摘要： Provided is a tryptophan-2,3-dioxygenase (TDO) and/or indoleamine-2,3-dioxygenase (IDO) inhibitor compound for use in medicine, which compound comprises the following formula: wherein X2, X4, X10, and X11 may be the same or different and each is independently selected from C and N; X1, X3, X5, X6, X7, X8, and X9 may be the same or different and each is independently selected from C, N and O; each bond having a dotted line may independently be a double bond or a single bond, provided that valencies at each atom are maintained; the dotted lines joining X4 with the carbon atoms either side of X2 are single bonds, and are only present when X2 is absent, X3 is absent and X4 is C, and when these bonds are present the ring carbons on each side of X2 are not directly bonded to each other; each R1 may be present or absent and may be the same or different and is selected from H and a substituted or unsubstituted organic group, provided that the number of R1 groups present is such that the valency of X1 is maintained; each R12, R13, R13′, R14, R15 and R15′ may be present or absent and may be the same or different and each is independently selected from H and a substituted or unsubstituted organic group, provided that the number of such R groups present is such that the valency of the ring carbon atoms is maintained; R16 may be present or absent and is selected from H and a substituted or unsubstituted organic group, provided that the number of R16 groups present is such that the valency of X2 is maintained; each R17 may be present or absent and may be the same or different and is independently selected from H and a substituted or unsubstituted organic group, provided that the number of R17 groups present is such that the valency of X3 is maintained; each R2, R3, R4, and R5 may be present or absent and may be the same or different and is selected from H and a substituted or unsubstituted organic group, provided that the number of such R groups present is such that the valencies of X6, X7, X8, and X9 are maintained; each R7, R8 and R9 may be present or absent and may be the same or different and is selected from H and a substituted or unsubstituted organic group, provided that the number of such R groups present is such that the valencies of X10, X11, and X5 are maintained; and R6 is selected from H and a substituted or unsubstituted organic group, preferably H and a substituted or unsubstituted C1-C6 alkyl group; and wherein any R group may form a ring with any other R group on an adjacent and/or proximal atom.

2. 发明授权

US10287252B2 Inhibitors of tryptophan-2,3-dioxygenase or indoleamine-2,3-dioxygenase 有权
公开(公告)号：US10287252B2
公开(公告)日：2019-05-14
申请号：US15524148
申请日：2015-11-02
申请人： IOmet Pharma Ltd.
发明人： Phillip M. Cowley , Alan Wise , Susan Davis , Margaret Huggett , Michael Kiczun
IPC分类号： C07D237/28 , A61K31/472 , A61K31/4725 , A61K31/502 , A61K45/06 , C07D217/02 , C07D405/12 , C07D409/12 , C07D413/12
摘要： Provided is a compound for use in medicine for inhibiting tryptophan-2,3-dioxygenase (TDO) and/or indoleamine-2,3-dioxygenase (IDO), which compound comprises formula (I) wherein X1, X2, and X7, may be the same or different and each is independently selected from C and N; X3, X4, X5, and X6 may be the same or different and each is independently selected from C, N, O and S wherein when X3 is N it has a double bond and wherein when X6 is N it has a double bond; the dotted line is a bond which may be present or absent; R1, R2, R3, R4, R5, R6, and R7 may be present or absent and may be the same or different and each is independently selected from H and a substituted or unsubstituted organic group, provided that at least one of R2, R3, R4 and R6 comprises a group Y; and provided that the number of R1, R2, R3, R4, R5, R6, and R7 groups present is such that the respective valencies of X1, X2, X3, X4, X5, X6, and X7 are maintained; and wherein Y is a group having a formula selected from (II), (III), (IV), (V) wherein L may be present or absent, and may be a substituted or unsubstituted organic linking group, and R31 and R32 may be the same or different and are selected from H and a substituted or unsubstituted organic group, X8 is selected from C and N, and each R313 may be the same or different and is selected from H and a substituted or unsubstituted organic group.

3. 发明授权

US10047074B2 Pharmaceutical compound 有权
公开(公告)号：US10047074B2
公开(公告)日：2018-08-14
申请号：US15504703
申请日：2015-08-13
申请人： IOmet Pharma Ltd.
发明人： Phillip M. Cowley , Alan Wise , Margaret Huggett
IPC分类号： C07D413/12 , C07D233/88 , C07D257/06 , C07D261/14 , C07D413/04 , A61K31/415 , A61K31/455 , A61K31/4164 , A61K31/4439 , A61K31/454 , C07D261/16 , A61K31/4155 , A61K31/41
摘要： Provided is a tryptophan-2,3-dioxygenase (TDO) and/or indoleamine-2,3-dioxygenase (IDO) inhibitor compound for use in medicine, which compound comprises the following formula (I): wherein X1 is selected from C and N; X3 and X5 may be the same or different and each is independently selected from C, N, O and S; Y is selected from N and O; Z is selected from C, N and O; each bond represented by a dotted line may independently be a double bond or a single bond, provided that valencies at each ring atom are maintained and provided that the ring Q contains at least one double bond and provided that the atom N has a double bond; R3 and R5 may be present or absent and may be the same or different and each is independently selected from H and a substituted or unsubstituted organic group, provided that the number of R3 groups present is such that the valency of X3 is maintained, and the number of R5 groups present is such that the valency of X5 is maintained; each R11 and R12 may be present or absent and may be the same or different and each is independently selected from H and a substituted or unsubstituted organic group, provided that the number of R11 and R12 groups present is such that the valency of Z is maintained; R21 is selected from H and a substituted or unsubstituted organic group; R22 may be present or absent and is selected from H and a substituted or unsubstituted organic group; and Cy is a cyclic organic group.

4. 发明授权

US09931347B2 Pharmaceutical compound 有权
公开(公告)号：US09931347B2
公开(公告)日：2018-04-03
申请号：US15100494
申请日：2014-12-02
申请人： IOmet Pharma Ltd.
发明人： Phillip Martin Cowley , Alan Wise , Margaret Huggett
IPC分类号： A61K31/551 , A61K31/404 , C07D401/04 , C07D403/12 , C07D401/12 , C07D403/04 , C07D405/12 , C07D413/12 , C07D471/04 , C07D487/04 , C07D209/34 , C07D209/40 , C07D513/04 , A61K31/435 , A61K31/4439 , A61K31/444 , A61K31/454 , A61K31/4545 , A61K31/4725 , A61K31/496 , A61K31/497 , A61K31/498 , A61K31/4985 , A61K31/506 , A61K31/5377 , A61K31/55 , A61K45/06 , C07D209/20 , C07D401/06 , C07D401/14 , C07D403/06 , C07D405/14 , C07D409/14 , C07D413/14 , C07D471/10
CPC分类号： A61K31/551 , A61K31/404 , A61K31/435 , A61K31/4439 , A61K31/444 , A61K31/454 , A61K31/4545 , A61K31/4725 , A61K31/496 , A61K31/497 , A61K31/498 , A61K31/4985 , A61K31/506 , A61K31/5377 , A61K31/55 , A61K45/06 , C07D209/20 , C07D209/34 , C07D209/40 , C07D401/04 , C07D401/06 , C07D401/12 , C07D401/14 , C07D403/04 , C07D403/06 , C07D403/12 , C07D405/12 , C07D405/14 , C07D409/14 , C07D413/12 , C07D413/14 , C07D471/04 , C07D471/10 , C07D487/04 , C07D513/04
摘要： Provided is a tryptophan-2,3-dioxygenase (TDO) and/or indoleamine-2,3-dioxygenase (IDO) inhibitor compound for use in medicine, which compound comprises the following formula: wherein X2, X4, X10, and X11 may be the same or different and each is independently selected from C and N; X1, X3, X5, X6, X7, X8, and X9 may be the same or different and each is independently selected from C, N and O; each bond having a dotted line may independently be a double bond or a single bond, provided that valencies at each atom are maintained; the dotted lines joining X4 with the carbon atoms either side of X2 are single bonds, and are only present when X2 is absent, X3 is absent and X4 is C, and when these bonds are present the ring carbons on each side of X2 are not directly bonded to each other; each R1 may be present or absent and may be the same or different and is selected from H and a substituted or unsubstituted organic group, provided that the number of R1 groups present is such that the valency of X1 is maintained; each R12, R13, R13′, R14, R15 and R15′ may be present or absent and may be the same or different and each is independently selected from H and a substituted or unsubstituted organic group, provided that the number of such R groups present is such that the valency of the ring carbon atoms is maintained; R16 may be present or absent and is selected from H and a substituted or unsubstituted organic group, provided that the number of R16 groups present is such that the valency of X2 is maintained; each R17 may be present or absent and may be the same or different and is independently selected from H and a substituted or unsubstituted organic group, provided that the number of R17 groups present is such that the valency of X3 is maintained; each R2, R3, R4, and R5 may be present or absent and may be the same or different and is selected from H and a substituted or unsubstituted organic group, provided that the number of such R groups present is such that the valencies of X6, X7, X8, and X9 are maintained; each R7, R8 and R9 may be present or absent and may be the same or different and is selected from H and a substituted or unsubstituted organic group, provided that the number of such R groups present is such that the valencies of X10, X11, and X5 are maintained; and R6 is selected from H and a substituted or unsubstituted organic group, preferably H and a substituted or unsubstituted C1-C6 alkyl group; and wherein any R group may form a ring with any other R group on an adjacent and/or proximal atom.

5. 发明申请

US20180037553A1 INHIBITORS OF TRYPTOPHAN-2,3-DIOXYGENASE OR INDOLEAMINE-2,3-DIOXYGENASE 审中-公开
公开(公告)号：US20180037553A1
公开(公告)日：2018-02-08
申请号：US15524148
申请日：2015-11-02
申请人： IOmet Pharma Ltd.
发明人： Phillip M. Cowley , Alan Wise , Susan Davis , Margaret Huggett , Michael Kiczun
IPC分类号： C07D237/28 , C07D405/12 , A61K45/06 , C07D413/12 , A61K31/4725 , A61K31/502 , C07D217/02 , C07D409/12
CPC分类号： C07D237/28 , A61K31/472 , A61K31/4725 , A61K31/502 , A61K45/06 , C07D217/02 , C07D405/12 , C07D409/12 , C07D413/12
摘要： Provided is a compound for use in medicine for inhibiting tryptophan-2,3-dioxygenase (TDO) and/or indoleamine-2,3-dioxygenase (IDO), which compound comprises formula (I) wherein X1, X2, and X7, may be the same or different and each is independently selected from C and N; X3, X4, X5, and X6 may be the same or different and each is independently selected from C, N, O and S wherein when X3 is N it has a double bond and wherein when X6 is N it has a double bond; the dotted line is a bond which may be present or absent; R1, R2, R3, R4, R5, R6, and R7 may be present or absent and may be the same or different and each is independently selected from H and a substituted or unsubstituted organic group, provided that at least one of R2, R3, R4 and R6 comprises a group Y; and provided that the number of R1, R2, R3, R4, R5, R6, and R7 groups present is such that the respective valencies of X1, X2, X3, X4, X5, X6, and X7 are maintained; and wherein Y is a group having a formula selected from (II), (III), (IV), (V) wherein L may be present or absent, and may be a substituted or unsubstituted organic linking group, and R31 and R32 may be the same or different and are selected from H and a substituted or unsubstituted organic group, X8 is selected from C and N, and each R313 may be the same or different and is selected from H and a substituted or unsubstituted organic group.

6. 发明申请

US20170267668A1 PHARMACEUTICAL COMPOUND 审中-公开
公开(公告)号：US20170267668A1
公开(公告)日：2017-09-21
申请号：US15504703
申请日：2015-08-13
申请人： IOmet Pharma Ltd.
发明人： Phillip M. COWLEY , Alan WISE , Margaret Huggett
IPC分类号： C07D413/12 , A61K31/415 , C07D413/04 , A61K31/4439 , A61K31/4164 , A61K31/4155 , A61K31/454 , C07D257/06 , A61K31/41 , C07D233/88 , C07D261/14 , C07D261/16
CPC分类号： C07D413/12 , A61K31/41 , A61K31/415 , A61K31/4155 , A61K31/4164 , A61K31/4192 , A61K31/4196 , A61K31/421 , A61K31/433 , A61K31/44 , A61K31/4439 , A61K31/454 , C07D233/88 , C07D257/06 , C07D261/14 , C07D261/16 , C07D413/04
摘要： Provided is a tryptophan-2,3-dioxygenase (TDO) and/or indoleamine-2,3-dioxygenase (IDO) inhibitor compound for use in medicine, which compound comprises the following formula (I): wherein X1 is selected from C and N; X3 and X5 may be the same or different and each is independently selected from C, N, O and S; Y is selected from N and O; Z is selected from C, N and O; each bond represented by a dotted line may independently be a double bond or a single bond, provided that valencies at each ring atom are maintained and provided that the ring Q contains at least one double bond and provided that the atom N has a double bond; R3 and R5 may be present or absent and may be the same or different and each is independently selected from H and a substituted or unsubstituted organic group, provided that the number of R3 groups present is such that the valency of X3 is maintained, and the number of R5 groups present is such that the valency of X5 is maintained; each R11 and R12 may be present or absent and may be the same or different and each is independently selected from H and a substituted or unsubstituted organic group, provided that the number of R11 and R12 groups present is such that the valency of Z is maintained; R21 is selected from H and a substituted or unsubstituted organic group; R22 may be present or absent and is selected from H and a substituted or unsubstituted organic group; and Cy is a cyclic organic group.

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