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1. 发明公开

US20230151069A1 Cyclic Peptides 审中-公开
公开(公告)号：US20230151069A1
公开(公告)日：2023-05-18
申请号：US17905894
申请日：2021-03-10
申请人： LIFEARC , Georg-August-Universität Göttingen Stiftung Öffentlichen Rechts Universitatsmedizin
发明人： Preeti BAKRANIA , David MATTHEWS , Elizabeth LOVE , Chido MPAMHANGA , Thomas BAYER , Mark CARR , Gareth HALL , Richard COWAN
IPC分类号： C07K14/47 , A61K39/00 , C07K16/18 , A61P25/28
CPC分类号： C07K14/4711 , A61K39/0007 , C07K16/18 , A61P25/28
摘要： The present invention relates to cyclized peptides based on amino acids 1-14 of amyloid-beta. The cyclic peptides are useful for inducing an immune response and as vaccines for the treatment of neurodegenerative diseases such as Alzheimer's disease.

2. 发明申请

US20210101999A1 Anti-Transglutaminase 2 Antibodies 有权
公开(公告)号：US20210101999A1
公开(公告)日：2021-04-08
申请号：US17121541
申请日：2020-12-14
申请人： LIFEARC
发明人： Tim Johnson , Phil Watson , David Matthews , Alex Brown
IPC分类号： C07K16/40 , A61K51/10
摘要： The invention provides antibodies and antigen-binding fragments thereof that selectively bind to an epitope within the core region of transglutaminase type 2 (TG2). Novel epitopes within the TG2 core are provided. The invention provides human TG2 inhibitory antibodies and uses thereof, particularly in medicine, for example in the treatment and/or diagnosis of conditions including Celiac disease, scarring, fibrosis-related diseases, neurodegenerative/neurological diseases and cancer.

3. 发明申请

US20180355060A1 Anti-Transglutaminase 2 Antibodies 审中-公开
公开(公告)号：US20180355060A1
公开(公告)日：2018-12-13
申请号：US15987611
申请日：2018-05-23
申请人： LIFEARC
发明人： Tim Johnson , Phil Watson , David Matthews , Alex Brown
IPC分类号： C07K16/40 , A61K51/10
CPC分类号： C07K16/40 , A61K51/1075 , A61K2039/505 , C07K2317/34 , C07K2317/40 , C07K2317/76
摘要： The invention provides antibodies and antigen-binding fragments thereof that selectively bind to an epitope within the core region of transglutaminase type 2 (TG2). Novel epitopes within the TG2 core are provided. The invention provides human TG2 inhibitory antibodies and uses thereof, particularly in medicine, for example in the treatment and/or diagnosis of conditions including Celiac disease, scarring, fibrosis-related diseases, neurodegenerative/neurological diseases and cancer.

4. 发明申请

US20200317753A1 Humanized Antibodies Against Enterovirus 71 审中-公开
公开(公告)号：US20200317753A1
公开(公告)日：2020-10-08
申请号：US16306496
申请日：2017-06-02
申请人： LIFEARC
发明人： Tilbe CREIGH-PULATMEN , Seema PATEL , David John MATTHEWS , Zhong HUANG
IPC分类号： C07K16/10 , A61K39/395 , A61K39/42 , G01N33/569 , A61P31/14
摘要： The present invention provides humanized antibodies against Enterovirus 71 (EV71), a causative agent of hand, foot, and mouth disease (HFMD), as well as pharmaceutical compositions comprising these antibodies and methods of their use in the treatment, prophylaxis, and diagnosis of HFMD. These antibodies are suitable for use in human subjects with HFMD or those at risk of HFMD, for example as a result of exposure to infected individuals.

5. 发明授权

US10669284B2 Fused thiazolopyrimidine derivatives as MNKS inhibitors 审中-公开
公开(公告)号：US10669284B2
公开(公告)日：2020-06-02
申请号：US15776536
申请日：2016-11-16
申请人： LIFEARC
发明人： Jon James Winter-Holt , Edward Giles Mciver , Martin Ambler , Stephen Lewis , Joanne Osborne , Kayleigh Webb-Smith
IPC分类号： C07D513/04 , C07D519/00 , A61K31/519 , A61K31/429 , A61P35/04
摘要： The present invention relates to compounds of formulae I and H, or pharmaceutically acceptable salts or esters thereof. Further aspects of the invention relate to pharmaceutical compositions and therapeutic uses of said compounds in the treatment of diseases of uncontrolled cell growth, proliferation and/or survival, inappropriate cellular immune responses, inappropriate cellular inflammatory responses, or neurodegenerative disorders, preferably tauopathies, even more preferably, Alzheimer's disease.

6. 发明申请

US20190352296A1 OXAZOLE DERIVATIVES FOR USE IN THE TREATMENT OF CANCER 审中-公开
公开(公告)号：US20190352296A1
公开(公告)日：2019-11-21
申请号：US16474120
申请日：2017-12-19
申请人： LIFEARC
发明人： Simon OSBORNE , Jonathan LARGE
IPC分类号： C07D413/14 , C07D413/12 , C07D487/04 , C07D417/12 , C07D417/14
摘要： A first aspect of the invention relates to a compound of formula (I), or a pharmaceutically acceptable salt or ester thereof, wherein: •B is an aryl or heteroaryl group optionally substituted by one or more R10 groups; and *X is selected from 0, (CR11R12)p and (CR11R12)p CO. Said compounds are capable of inhibiting PAICS and are useful in the treatment of proliferative disorders. Further aspects relate to pharmaceutical compositions, therapeutic uses and process for preparing compounds of formula (I).

7. 发明申请

US20180346469A1 Pyrropyrimidine Compounds As MNKS Inhibitors 审中-公开
公开(公告)号：US20180346469A1
公开(公告)日：2018-12-06
申请号：US15776574
申请日：2016-11-16
申请人： LIFEARC
发明人： Jon James Winter-Holt , Edward Giles Mciver , Stephen Lewis , Joanne Osborne
IPC分类号： C07D487/04 , A61K31/519 , A61K45/06
CPC分类号： C07D487/04 , A61K31/519 , A61K45/06 , A61K2300/00
摘要： The present invention relates to compounds of formulae I, or pharmaceutically acceptable salts or esters thereof, wherein: R1 is selected from H and CO—NR8R9, wherein R8 and R9 are each independently selected from H, alkyl, cycloalkyl and mono or bicyclic heterocycloalkyl, wherein said alkyl group is optionally substituted by one or more R12 groups, and said heterocycloalkyl is optionally substituted by R10 or R12; or R8 and R9 are linked, together with the nitrogen to which they are attached, to form a heterocycloalkyl group optionally containing one or more additional heteroatoms, and optionally substituted by one or more groups select from R10 and (CH2)mR12; R2 is selected from H and alkyl, wherein said alkyl group is optionally substituted by one or more R12 groups; R3 is selected from alkyl, cycloalkyl and heterocycloalkyl, each of which may be optionally substituted by halo, OH or alkoxy; Z1, Z2, Z3 and Z4 are all C; R4, R5, R6 and R7 are each independently selected from H, alkyl, CN, NO2,OH, alkoxy, NHCO-alkyl, halo and haloalkyl; or Z1, Z3 and Z4 are all C, Z2 is N, R5 is absent and R4, R6 and R7 are as defined above; or Z1, Z3 and Z4 are all C, Z1 is N, R4 is absent and R5, R6 and R7 are as defmed above; each R10 and R11 is independently alkyl; each R12 is independently selected from CO2R10, COOH, OH, alkoxy, haloalkyl, NH2, NHR10, NR10R11, heteroaryl and heterocycloalkyl; R13 is H or halo. Further aspects relate to pharmaceutical compositions and therapeutic uses of said compounds in the treatment of diseases of uncontrolled cell growth, proliferation and/or survival, inappropriate cellular immune responses, inappropriate cellular inflammatory responses, or neurodegenerative disorders, preferably tauopathies, even more preferably, Alzheimer's disease.

8. 发明授权

US11136338B2 Fused thiazolopyrimidine derivatives as MNKs inhibitors 有权
公开(公告)号：US11136338B2
公开(公告)日：2021-10-05
申请号：US16855701
申请日：2020-04-22
申请人： LIFEARC
发明人： Jon James Winter-Holt , Edward Giles Mciver , Martin Ambler , Stephen Lewis , Joanne Osborne , Kayleigh Webb-Smith
IPC分类号： C07D513/04 , C07D519/00 , A61K31/519 , A61K31/429 , A61P35/04
摘要： The present invention relates to compounds of formulae I and H, or pharmaceutically acceptable salts or esters thereof. Further aspects of the invention relate to pharmaceutical compositions and therapeutic uses of said compounds in the treatment of diseases of uncontrolled cell growth, proliferation and/or survival, inappropriate cellular immune responses, inappropriate cellular inflammatory responses, or neurodegenerative disorders, preferably tauopathies, even more preferably. Alzheimer's disease.

9. 发明授权

US10961233B2 Oxazole derivatives for use in the treatment of cancer 有权
公开(公告)号：US10961233B2
公开(公告)日：2021-03-30
申请号：US16474114
申请日：2017-12-19
申请人： LIFEARC
发明人： Simon Osborne , Jonathan Large
IPC分类号： C07D413/12 , C07D413/14 , C07D263/48
摘要： A first aspect of the invention relates to a compound of formula (I), or a pharmaceutically acceptable salt or ester thereof, • B is a saturated or partially unsaturated monocyclic or bicyclic, heterocyclic group optionally substituted by one or more R 10 groups; *X is selected from SO2, CO2, CO, CONR11 and (CR12R13) p. Said compounds are capable of inhibiting PAICS and are useful in the treatment of proliferative disorders. Further aspects relate to pharmaceutical compositions, therapeutic uses and process for preparing compounds of formula (I).

10. 发明申请

US20200247822A1 Fused Thiazolopyrimidine Derivatives As MNKS Inhibitors 审中-公开
公开(公告)号：US20200247822A1
公开(公告)日：2020-08-06
申请号：US16855701
申请日：2020-04-22
申请人： LIFEARC
发明人： Jon James Winter-Holt , Edward Giles Mciver , Martin Ambler , Stephen Lewis , Joanne Osborne , Kayleigh Webb-Smith
IPC分类号： C07D513/04 , A61P35/04 , C07D519/00 , A61K31/429 , A61K31/519
摘要： The present invention relates to compounds of formulae I and H, or pharmaceutically acceptable salts or esters thereof. Further aspects of the invention relate to pharmaceutical compositions and therapeutic uses of said compounds in the treatment of diseases of uncontrolled cell growth, proliferation and/or survival, inappropriate cellular immune responses, inappropriate cellular inflammatory responses, or neurodegenerative disorders, preferably tauopathies, even more preferably. Alzheimer's disease.

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