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公开(公告)号:US20190185478A1
公开(公告)日:2019-06-20
申请号:US16226398
申请日:2018-12-19
Applicant: Agency for Science, Technology and Research
Inventor: Jenefer Alam , Soo Yei Ho , Wei Ling Wang , Athisayamani Jeyaraj Duraiswamy
IPC: C07D487/04
CPC classification number: C07D487/04
Abstract: The present invention relates to compounds of formula (I), combinations and uses thereof for disease therapy, or a pharmaceutically acceptable salt, solvate or polymorph thereof, including all tautomers and stereoisomers thereof wherein R1 represents H; optionally substituted alkyl (wherein optional substituents include one or more substituents each independently selected from C1-6alkoxy, NH2, —NHC1-3alkyl and —N(C1-3alkyl)2); —C(O)Oalkyl; haloalkyl; haloalkoxy; or -alkylaryl; each R2 independently represents H; optionally substituted alkyl (wherein optional substituents include one or more substituents each independently selected from C1-6alkoxy, NH2, —NHC1-3alkyl and —N(C1-3alkyl)2); -alkylaryl; optionally substituted carbocyclyl (wherein optional substituents include one or more substituents each independently selected from C1-6alkyl, C1-6alkoxy, C1-6haloalkyl, C1-6haloalkoxy and halo); optionally substituted heterocyclyl (wherein optional substituents include one or more substituents each independently selected from C1-6alkyl, C1-6alkoxy, —C(O)OC1-6alkyl, —C(O)C1-6alkyl and —C(O)NHC1-6alkyl); —NHalkyl; —N(alkyl)2; amino; hydroxyl; alkoxy or halo; n represents 0, 1 or 2; R3 represents H or alkyl; R4 represents H or alkyl; R5 represents H or alkyl; W and X each independently represent C═O; C═S; or CH2; Y represents aryl; heteroaryl; optionally substituted carbocyclyl (wherein optional substituents include one or more substituents each independently selected from C1-6alkyl, C1-6alkoxy, C1-6haloalkyl, C1-6haloalkoxy and halo); or optionally substituted heterocyclyl (wherein optional substituents include one or more substituents each independently selected from C1-6alkyl, C1-6alkoxy, —C(O)OC1-6alkyl, —C(O)C1-6alkyl and —C(O)NHC1-6alkyl); and Z represents optionally substituted alkyl (wherein optional substituents include one or more substituents each independently selected from C1-6alkoxy, NH2, —NHC1-3alkyl and —N(C1-3alkyl)2); aryl; heteroaryl; -alkylaryl;-alkylheteroaryl; optionally substituted carbocyclyl (wherein optional substituents include one or more substituents each independently selected from C1-6alkyl, C1-6alkoxy, C1-6haloalkyl, C1-6haloalkoxy and halo); optionally substituted heterocyclyl (wherein optional substituents include one or more substituents each independently selected from C1-6alkyl, C1-6alkoxy, —C(O)OC1-6alkyl, —C(O)C1-6alkyl and —C(O)NHC1-6alkyl); -alkylcarbocyclyl wherein carbocyclyl is optionally substituted (wherein optional substituents include one or more substituents each independently selected from C1-6alkyl, C1-6alkoxy, C1-6haloalkoxy and halo); -alkylheterocyclyl wherein heterocyclyl is optionally substituted (wherein optional substituents include one or more substituents each independently selected from C1-6alkyl, —C(O)OC1-6alkyl, —C(O)C1-6alkyl and —C(O)NHC1-6alkyl); -arylcarbocyclyl wherein carbocyclyl is optionally substituted (wherein optional substituents include one or more substituents each independently selected from C1-6alkyl, C1-6alkoxy, C1-6haloalkoxy and halo); or -arylheterocyclyl wherein heterocyclyl is optionally substituted (wherein optional substituents include one or more substituents each independently selected from C1-6alkyl, —C(O)OC1-6alkyl, —C(O)C1-6alkyl and —C(O)NHC1-6alkyl).
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公开(公告)号:US20180170932A1
公开(公告)日:2018-06-21
申请号:US15899675
申请日:2018-02-20
Applicant: Agency for Science, Technology and Research
Inventor: Soo Yei Ho , Stephanie Eliane BLANCHARD , Athisayamani Jeyaraj DURAISWAMY , Jenefer ALAM , Vikrant Arun ADSOOL
IPC: C07D473/06 , C07D473/08 , A61K31/522 , A61K31/5377
Abstract: The invention relates to the use of compounds of general structure (I) in modulation of the Wnt pathway [Formula should be inserted here] wherein R1, R2, R3, R4 and R5 are each, independently, H or an alkyl group; D is selected from the group consisting of H, halogen, alkyl, cycloalkyl, aryl, and dialkylamino, each (other than H and halogen) being optionally substituted; Ar is an aryl or heteroaryl group, optionally substituted; Cy is an aryl, heteroaryl or a saturated ring containing at least one heteroatom, each being optionally substituted; and n is an integer from 1 to 3.
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公开(公告)号:US11555037B2
公开(公告)日:2023-01-17
申请号:US17100474
申请日:2020-11-20
Applicant: Agency for Science, Technology and Research
Inventor: Soo Yei Ho , Stephanie Eliane Blanchard , Athisayamani Jeyaraj Duraiswamy , Jenefer Alam , Vikrant Arun Adsool
IPC: C07D473/06 , A61K31/522 , A61K31/5377 , C07D473/08
Abstract: The invention relates to the use of compounds of general structure (I) in modulation of the Wnt pathway wherein R1, R2, R3, R4 and R5 are each, independently, H or an alkyl group; D is selected from the group consisting of H, halogen, alkyl, cycloalkyl, aryl, and dialkylamino, each (other than H and halogen) being optionally substituted; Ar is an aryl or heteroaryl group, optionally substituted; Cy is an aryl, heteroaryl or a saturated ring containing at least one heteroatom, each being optionally substituted; and n is an integer from 1 to 3.
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公开(公告)号:US11834430B2
公开(公告)日:2023-12-05
申请号:US16646693
申请日:2018-09-12
Applicant: AGENCY FOR SCIENCE, TECHNOLOGY AND RESEARCH
Inventor: Soo Yei Ho , Anders Poulsen , Sum Wai Eldwin Tan , Shi Hua Ang , Thomas Hugo Keller
IPC: C07D401/04 , C07D231/12 , C07D233/12 , C07D249/08 , C07D401/12 , C07D401/14 , A61P35/00 , C07D233/06 , C07D233/60 , C07D261/08 , C07D277/24 , C07D403/12
CPC classification number: C07D401/04 , A61P35/00 , C07D231/12 , C07D233/06 , C07D233/60 , C07D249/08 , C07D261/08 , C07D277/24 , C07D401/12 , C07D401/14 , C07D403/12
Abstract: The present invention relates to compounds of general Formula (I), and/or tautomers, enantiomers, solvates, hydrates, and pharmaceutically acceptable salts thereof. The present invention also relates to compounds of Formula (I) for use in therapy, methods of treating isoprenylcysteine carboxyl methyltransferase (ICMT) related disorders or uses of compounds of Formula (I) in the manufacture of a medicament for the treatment of ICMT-related disorders, wherein the disorder is cancer and/or progeria. The present invention further relates to processes for synthesizing compounds of Formula (I).
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公开(公告)号:US20210155623A1
公开(公告)日:2021-05-27
申请号:US17100474
申请日:2020-11-20
Applicant: Agency for Science, Technology and Research
Inventor: Soo Yei Ho , Stephanie Eliane BLANCHARD , Athisayamani Jeyaraj DURAISWAMY , Jenefer ALAM , Vikrant Arun ADSOOL
IPC: C07D473/06 , A61K31/522 , A61K31/5377 , C07D473/08
Abstract: The invention relates to the use of compounds of general structure (I) in modulation of the Wnt pathway wherein R1, R2, R3, R4 and R5 are each, independently, H or an alkyl group; D is selected from the group consisting of H, halogen, alkyl, cycloalkyl, aryl, and dialkylamino, each (other than H and halogen) being optionally substituted; Ar is an aryl or heteroaryl group, optionally substituted; Cy is an aryl, heteroaryl or a saturated ring containing at least one heteroatom, each being optionally substituted; and n is an integer from 1 to 3.
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公开(公告)号:US20210130317A1
公开(公告)日:2021-05-06
申请号:US16646693
申请日:2018-09-12
Applicant: AGENCY FOR SCIENCE, TECHNOLOGY AND RESEARCH
Inventor: Soo Yei Ho , Anders Poulsen , Sum Wai Eldwin Tan , Shi Hua Ang , Thomas Hugo Keller
IPC: C07D401/04 , C07D249/08 , C07D233/60 , C07D277/24 , C07D401/12 , C07D231/12 , C07D233/06 , C07D261/08 , C07D401/14 , C07D403/12 , A61P35/00
Abstract: The present invention relates to compounds of general Formula (I), and/or tautomers, enantiomers, solvates, hydrates, and pharmaceutically acceptable salts thereof. The present invention also relates to compounds of Formula (I) for use in therapy, methods of treating isoprenylcysteine carboxyl methyltransferase (ICMT) related disorders or uses of compounds of Formula (I) in the manufacture of a medicament for the treatment of ICMT-related disorders, wherein the disorder is cancer and/or progeria. The present invention further relates to processes for synthesizing compounds of Formula (I).
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公开(公告)号:US20210047336A1
公开(公告)日:2021-02-18
申请号:US17084507
申请日:2020-10-29
Applicant: Agency for Science, Technology and Research
Inventor: Jenefer Alam , Soo Yei Ho , Wei Ling Wang , Athisayamani Jeyaraj Duraiswamy
IPC: C07D487/04 , A61K31/519 , A61P35/04 , A61P35/00
Abstract: The present invention relates to compounds of formula (I), combinations and uses thereof for disease therapy, or a pharmaceutically acceptable salt, solvate or polymorph thereof, including all tautomers and stereoisomers thereof wherein R1 represents H; optionally substituted alkyl (wherein optional substituents include one or more substituents each independently selected from C1-6alkoxy, NH2, —NHC1-3alkyl and —N(C1-3alkyl)2); —C(O)Oalkyl; haloalkyl; haloalkoxy; or -alkylaryl; each R2 independently represents H; optionally substituted alkyl (wherein optional substituents include one or more substituents each independently selected from C1-6alkoxy, NH2, —NHC1-3alkyl and —N(C1-3alkyl)2); -alkylaryl; optionally substituted carbocyclyl (wherein optional substituents include one or more substituents each independently selected from C1-6alkyl, C1-6alkoxy, C1-6haloalkyl, C1-6haloalkoxy and halo); optionally substituted heterocyclyl (wherein optional substituents include one or more substituents each independently selected from C1-6alkyl, C1-6alkoxy, —C(O)OC1-6alkyl, —C(O)C1-6alkyl and —C(O)NHC1-6alkyl); —NHalkyl; —N(alkyl)2; amino; hydroxyl; alkoxy or halo; n represents 0, 1 or 2; R3 represents H or alkyl; R4 represents H or alkyl; R5 represents H or alkyl; W and X each independently represent C═O; C═S; or CH2; Y represents aryl; heteroaryl; optionally substituted carbocyclyl (wherein optional substituents include one or more substituents each independently selected from C1-6alkyl, C1-6alkoxy, C1-6haloalkyl, C1-6haloalkoxy and halo); or optionally substituted heterocyclyl (wherein optional substituents include one or more substituents each independently selected from C1-6alkyl, C1-6alkoxy, —C(O)OC1-6alkyl, —C(O)C1-6alkyl and —C(O)NHC1-6alkyl); and Z represents optionally substituted alkyl (wherein optional substituents include one or more substituents each independently selected from C1-6alkoxy, NH2, —NHC1-3alkyl and —N(C1-3alkyl)2); aryl; heteroaryl; -alkylaryl; -alkylheteroaryl; optionally substituted carbocyclyl (wherein optional substituents include one or more substituents each independently selected from C1-6alkyl, C1-6alkoxy, C1-6haloalkyl, C1-6haloalkoxy and halo); optionally substituted heterocyclyl (wherein optional substituents include one or more substituents each independently selected from C1-6alkyl, C1-6alkoxy, —C(O)OC1-6alkyl, —C(O)C1-6alkyl and —C(O)NHC1-6alkyl); -alkylcarbocyclyl wherein carbocyclyl is optionally substituted (wherein optional substituents include one or more substituents each independently selected from C1-6alkyl, C1-6alkoxy, C1-6haloalkoxy and halo); -alkylheterocyclyl wherein heterocyclyl is optionally substituted (wherein optional substituents include one or more substituents each independently selected from C1-6alkyl, —C(O)OC1-6alkyl, —C(O)C1-6alkyl and —C(O)NHC1-6alkyl); -arylcarbocyclyl wherein carbocyclyl is optionally substituted (wherein optional substituents include one or more substituents each independently selected from C1-6alkyl, C1-6alkoxy, C1-6haloalkoxy and halo); or -arylheterocyclyl wherein heterocyclyl is optionally substituted (wherein optional substituents include one or more substituents each independently selected from C1-6alkyl, —C(O)OC1-6alkyl, —C(O)C1-6alkyl and —C(O)NHC1-6alkyl).
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公开(公告)号:US11434245B2
公开(公告)日:2022-09-06
申请号:US17084507
申请日:2020-10-29
Applicant: Agency for Science, Technology and Research
Inventor: Jenefer Alam , Soo Yei Ho , Wei Ling Wang , Athisayamani Jeyaraj Duraiswamy
IPC: A61K31/519 , A61P19/04 , C07D487/04 , A61P35/04 , A61P35/00
Abstract: The present invention relates to compounds of formula (I), combinations and uses thereof for disease therapy, or a pharmaceutically acceptable salt, solvate or polymorph thereof, including all tautomers and stereoisomers thereof wherein.
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公开(公告)号:US09981964B2
公开(公告)日:2018-05-29
申请号:US15105312
申请日:2014-12-17
Applicant: Agency for Science, Technology and Research
Inventor: Jenefer Alam , Anders Poulsen , Soo Yei Ho , Wei Ling Wang , Athisayamani Jeyaraj Duraiswamy
IPC: C07D471/04 , C07D487/04
CPC classification number: C07D471/04 , C07D487/04
Abstract: The present invention relates to compounds of formula (I), combinations and uses thereof for disease therapy, or a pharmaceutically acceptable salt, solvate or polymorph thereof, including all tautomers and stereoisomers thereof wherein R1 represents optionally substituted alkyl (wherein optional substituents include one or more substituents each independently selected from C1-6alkoxy); optionally substituted carbocyclyl (wherein optional substituents include one or more substituents each independently selected from C1-6alkyl, C1-6alkoxy, C1-6haloalkyl, C1-6haloalkoxy and halo); or -alkylaryl; R2 represents H; or alkyl; R3 represents H; or alkyl; U, V and W represent —(CH2)—; or U and V together represent —CH═CH— and W represents C═O; Y represents aryl; heteroaryl; optionally substituted carbocyclyl (wherein optional substituents include one or more substituents each independently selected from C1-6alkyl, C1-6alkoxy, C1-6haloalkyl, C1-6haloalkoxy and halo); or optionally substituted heterocyclyl (wherein optional substituents include one or more substituents each independently selected from C1-6alkyl, C1-6 alkoxy, —C(O)OC1-6alkyl, —C(O)C1-6alkyl and —C(O)NHC1-6alkyl); and Z represents aryl; heteroaryl; optionally substituted carbocyclyl (wherein optional substituents include one or more substituents each independently selected from C1-6alkyl, C1-6alkoxy, C1-6haloalkyl, C1-6haloalkoxy and halo); or optionally substituted heterocyclyl (wherein optional substituents include one or more substituents each independently selected from C1-6alkyl, C1-6 alkoxy, —C(O)OC1-6alkyl, —C(O)C1-6alkyl and —C(O)NHC1-6alkyl).
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公开(公告)号:US09926320B2
公开(公告)日:2018-03-27
申请号:US14893172
申请日:2014-05-19
Applicant: Agency for Science, Technology and Research
Inventor: Soo Yei Ho , Stephanie Eliane Blanchard , Athisayamani Jeyaraj Duraiswamy , Jenefer Alam , Vikrant Arun Adsool
IPC: A61K31/522 , C07D473/06 , A61K31/5377 , C07D473/08
CPC classification number: C07D473/06 , A61K31/522 , A61K31/5377 , C07D473/08
Abstract: The invention relates to the use of compounds of general structure (I) in modulation of the Wnt pathway [Formula should be inserted here] wherein R1, R2, R3, R4 and R5 are each, independently, H or an alkyl group; D is selected from the group consisting of H, halogen, alkyl, cycloalkyl, aryl, and dialkylamino, each (other than H and halogen) being optionally substituted; Ar is an aryl or heteroaryl group, optionally substituted; Cy is an aryl, heteroaryl or a saturated ring containing at least one heteroatom, each being optionally substituted; and n is an integer from 1 to 3.
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