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1.发明申请公开(公告)号：US20170121316A1
公开(公告)日：2017-05-04
申请号：US15315326
申请日：2015-03-30
Inventor： Xabier AGUIRRE ENA , Julen OYARZABAL SANTAMARINA , Felipe PRÓSPER CARDOSO , Maria Obdulia RABAL GRACIA , Juan Roberto RODRÍGUEZ MADOZ , Edurne SAN JOSÉ ENÉRIZ
IPC: C07D405/14 , C07D401/12
CPC classification number: C07D405/14 , C07D215/42 , C07D401/04 , C07D401/12 , C07D401/14
Abstract: It relates to the use of compounds of formula (I′), or their pharmaceutically or veterinary acceptable salts, or their stereoisomers or mixtures thereof, as anticancer agents and as agents for generating induced pluripotent stem cells. Compounds of formula (I′), wherein R2′ is an alcoxy group, a hydrocarbon chain or a ring system, and R1, R3, and R4 are as defined herein, are dual inhibitors of histone methyltransferases and DNA methyltransferases. It also relates to the compounds of formula (I′), or their pharmaceutically or veterinary acceptable salts, or their stereoisomers or mixtures thereof, wherein R2′ is phenyl or 5- to 6-membered heteroaromatic ring, both optionally fused to another rings (i.e., compounds of formula (I)). It also relates to pharmaceutical or veterinary compositions containing compounds of formula (I).
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公开(公告)号：US20170217973A1
公开(公告)日：2017-08-03
申请号：US15501814
申请日：2015-08-03
Inventor： María del Mar CUADRADO TEJEDOR , Ana Maria GARCÍA OSTA , Julen OYARZABAL SANTAMARINA , Maria Obdulia RABAL GRACIA , Juan Antonio SÁNCHEZ ARIAS , Ana UGARTE BAZTÁN
IPC: C07D487/04
CPC classification number: C07D487/04
Abstract: Novel compounds for use in cognition improvement It relates to certain compounds having a polycyclic structure and a —(C═O)NRaRb moiety, wherein the polycyclic structure comprises at least three ring systems, wherein one ring system is a polycyclic ring system comprising from 2 to 4 rings; at least one ring is an aromatic ring; and wherein the structure comprises at least 3 nitrogen atoms and 1 oxygen atom. It also relates to pharmaceutical compositions containing them, and to their use in medicine, in particular in the treatment and/or prevention of neurological disorders coursing with a cognition deficit or impairment, or neared-generative diseases.
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公开(公告)号：US20200317733A1
公开(公告)日：2020-10-08
申请号：US16853397
申请日：2020-04-20
Inventor： Inés Noelia CASARES LAGAR , Juan José LASARTE SAGASTIBELZA , Teresa LOZANO MOREDA , Julen OYARZABAL SANTAMARINA , Maria Obdulia RABAL GRACIA
Abstract: The present invention provides peptides of general formula (I) and salts thereof, wherein: R1 and R2, taken together, form a birradical linker; and R2′ is hydrogen; or, alternatively, R1 is selected from hydrogen, —C(═O)—CH2—NH—C(═O)—(C1-C5)alkyl, and —C(═O)—(C1-C20)alkyl; one of R2 and R2′ is hydrogen and the other is selected from —C(═O)NR3R4, and —C(═O)OH; and R3 and R4 are same or different and are selected from hydrogen and (C1-C10)alkyl. These peptides are highly efficient in binding and inhibiting FoxP3, being efficient in inhibiting and blocking Treg cell functionality, which make them useful in the treatment of cancer. The present invention also provides constructs comprising the peptide of formula (I) as well as combinations comprising the peptide of formula (I), the construct or both.
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Patent Agency Ranking
公开(公告)号：US20180362525A1
公开(公告)日：2018-12-20
申请号：US15775746
申请日：2016-11-15
Inventor： Xabier AGUIRRE ENA , Julen OYARZABAL SANTAMARINA , Felipe PRÓSPER CARDOSO , Maria Obdulia RABAL GRACIA , Edurne SAN JOSÉ ENÉRIZ , Juan Antonio SÁNCHEZ ARIAS
IPC: C07D471/04 , A61P35/02
CPC classification number: C07D471/04 , A61P35/02
Abstract: It relates to the compounds of formula (I), or their pharmaceutically or veterinary acceptable salts, or their stereoisomers or mixtures thereof, wherein A, R1, R2, and R3 are as defined herein, which are inhibitors of one or more DNMTs selected from the group consisting of DNMT1, DNMT3A and DNMT3B. It also relates to pharmaceutical or veterinary compositions containing them, and to their use in medicine, in particular in the treatment and/or prevention of cancer, fibrosis and/or immunomodulation.
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公开(公告)号：US20170231931A1
公开(公告)日：2017-08-17
申请号：US15504281
申请日：2015-08-25
Inventor： María del Mar CUADRADO TEJEDOR , Ana María GARCÍA OSTA , Julen OYARZABAL SANTAMARINA , Maria Obdulia RABAL GRACIA
IPC: A61K31/167 , A61K31/519 , A61K31/4985 , A61K31/53
CPC classification number: A61K31/167 , A61K31/4985 , A61K31/519 , A61K31/53 , A61K45/06 , A61K2300/00
Abstract: The invention relates to a product that comprises a compound of formula (1-01) to (1-47) and a compound of formula (2-01) to (2-26), or their pharmaceutically or veterinary acceptable salts thereof, or any stereoisomers either of the compounds or of any of their pharmaceutically or veterinary acceptable salts. The invention also relates to said product for use in the treatment and/or prevention of a neurological disorder coursing with a cognition deficit or impairment, or a neurodegenerative disease.
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公开(公告)号：US20190276496A1
公开(公告)日：2019-09-12
申请号：US16343394
申请日：2017-10-19
Inventor： Inés Noelia CASARES LAGAR , Juan José LASARTE SAGASTIBELZA , Teresa LOZANO MOREDA , Julen OYARZABAL SANTAMARINA , Maria Obdulia RABAL GRACIA
Abstract: The present invention provides peptides of general formula (I) and salts thereof, wherein: R1 and R2, taken together, form a birradical linker; and R2′ is hydrogen; or, alternatively, R1 is selected from hydrogen, —C(═O)—CH2—NH—C(═O)—(C1-C5)alkyl, and —C(═O)—(C1-C20)alkyl; one of R2 and R2′ is hydrogen and the other is selected from —C(═O)NR3R4, and —C(═O)OH; and R3 and R4 are same or different and are selected from hydrogen and (C1-C10)alkyl. These peptides are highly efficient in binding and inhibiting FoxP3, being efficient in inhibiting and blocking Treg cell functionality, which make them useful in the treatment of cancer. The present invention also provides constructs comprising the peptide of formula (I) as well as combinations comprising the peptide of formula (I), the construct or both.
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公开(公告)号：US20190127354A1
公开(公告)日：2019-05-02
申请号：US16061325
申请日：2016-12-13
Inventor： Xabier AGUIRRE ENA , Julen OYARZABAL SANTAMARINA , Felipe PRÓSPER CARDOSO , Maria Obdulia RABAL GRACIA , Edurne SAN JOSÉ ENÉRIZ , Juan Antonio SÁNCHEZ ARIAS
IPC: C07D405/14 , C07D401/14 , C07D405/04 , A61P35/00
Abstract: It relates to the compounds of formula (I), or their pharmaceutically or veterinary acceptable salts, or their stereoisomers or mixtures of stereoisomers, wherein R is a radical selected from the group consisting of formula (A), formula (B), formula (C), formula (D), and formula (E), and R1, R2, and R3 are as defined herein, which are inhibitors of one or more DNMTs selected from the group consisting of DNMT1, DNMT3A and DNMT3B. It also relates to pharmaceutical or veterinary compositions containing them, and to their use in medicine, in particular in the treatment and/or prevention of cancer, fibrosis and/or immunomodulation.
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8.发明申请NOVEL COMPOUNDS AS DUAL INHIBITORS OF PHOSPHODIESTERASES AND HISTONE DEACETYLASES 有权新型化合物作为磷酸二氢钠和组胺脱乙酰壳多糖的双重抑制剂公开(公告)号：US20160002246A1
公开(公告)日：2016-01-07
申请号：US14770065
申请日：2014-02-27
Inventor： Maria Del Mar CUADRADO TEJEDOR , Rafael FRANCO FERNÁNDEZ , Ana Maria GARCÍA OSTA , Julen OYARZABAL SANTAMARINA , Maria Obdulia RABAL GRACIA
IPC: C07D487/04 , C07D487/14
CPC classification number: C07D487/04 , A61K31/519 , C07D213/81 , C07D401/12 , C07D401/14 , C07D471/04 , C07D487/14
Abstract: It relates to certain compounds having a polycyclic structure and a hydroxamic acid moiety, wherein the polycyclic structure comprises at least three ring systems, wherein one ring system is a polycyclic ring system comprising from 2 to 4 rings; at least one ring is an aromatic ring; and wherein the structure comprises at least 3 nitrogen atoms and 1 oxygen atom. It also relates to a process for their preparation, as well as to pharmaceutical compositions containing them, and to their use in medicine, in particular in the treatment and/or prevention of neurological disorders coursing with a cognition deficit or impairment, or neurodegenerative diseases. wherein B1 is a radical selected from the group consisting of formula (A″), formula (B″), formula (C″), and formula (D″):
Abstract translation: 它涉及具有多环结构和异羟肟酸部分的某些化合物，其中多环结构包含至少三个环系，其中一个环系是包含2至4个环的多环系统; 至少一个环是芳环; 并且其中所述结构包含至少3个氮原子和1个氧原子。 它还涉及其制备方法，以及含有它们的药物组合物，以及它们在医药中的用途，特别是在用认知缺陷或损伤或神经变性疾病治疗和/或预防神经障碍方面的用途。 其中B1是选自式（A“），式（B”），式（C“）和式（D”）的基团：
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