公开(公告)号：US10927072B2

公开(公告)日：2021-02-23

申请号：US16516747

申请日：2019-07-19

申请人： Acetylon Pharmaceuticals, Inc.

发明人： John H. van Duzer ,  Ralph Mazitschek

IPC分类号： C07C259/10 ,  A61P25/14 ,  A61P25/28 ,  A61P25/00 ,  A61P25/16 ,  A61P35/00 ,  C07D213/81 ,  C07D309/14 ,  C07D413/12 ,  C07D417/12

摘要： The present invention relates to pyrimidine hydroxy amide compounds, the use of such compounds in the inhibition of HDAC6, and the use of such compounds in the treatment of various diseases, disorders, or conditions related to HDAC6.

公开(公告)号：US20190282573A1

公开(公告)日：2019-09-19

申请号：US16463140

申请日：2017-11-21

申请人： Acetylon Pharmaceuticals, Inc.

发明人： Steven Quayle ,  Simon Stewart Jones ,  Teru Hideshima ,  Kenneth C. Anderson

IPC分类号： A61K31/505 ,  A61K31/573 ,  C07K16/28 ,  A61K31/454 ,  A61P35/00

摘要： The present disclosure relates to a pharmaceutical combination comprising (a) a histone deacetylase 6 inhibitor and (b) a programmed death ligand 1 (PD-L1) inhibitor, including combined preparations and pharmaceutical compositions thereof; uses of such combination in the treatment or prevention of cancer; and methods of treating or preventing cancer in a subject comprising administering a therapeutically effective amount of such combination.

公开(公告)号：US10144714B2

公开(公告)日：2018-12-04

申请号：US15176826

申请日：2016-06-08

申请人： Acetylon Pharmaceuticals, Inc.

发明人： Farzaneh Seyedi ,  John H. van Duzer

IPC分类号： C07D239/42 ,  C07D239/30

摘要： The present invention relates to methods and intermediates useful for the synthesis of protein deacetylase inhibitors.

公开(公告)号：US10040769B2

公开(公告)日：2018-08-07

申请号：US15335971

申请日：2016-10-27

申请人： ACETYLON PHARMACEUTICALS, INC.

发明人： Olga Golonzhka ,  Matthew B. Jarpe

IPC分类号： C07D239/42 ,  A61K31/164 ,  A61K31/337 ,  A61K31/495 ,  A61K31/505

摘要： The invention relates to HDAC inhibitors for use in the treatment of diabetic peripheral neuropathy in a subject in need thereof. Also provided herein are methods for treating diabetic peripheral neuropathy in a subject in need thereof comprising administering to the subject a therapeutically effective amount of an HDAC inhibitor.

公开(公告)号：US20170327895A1

公开(公告)日：2017-11-16

申请号：US15497397

申请日：2017-04-26

申请人： Acetylon Pharmaceuticals, Inc.

发明人： Min Yang ,  Simon Steward Jones

IPC分类号： C12Q1/68 ,  G01N33/574

CPC分类号： C12Q1/6886 ,  C12Q2600/106 ,  C12Q2600/156 ,  C12Q2600/158 ,  G01N33/57415 ,  G01N2333/71

摘要： The invention relates to methods for using biomarkers to identify cancer patients that will or are likely to respond to treatment. Specifically, the invention relates to the use of one or more of three association studies of cancer types, gene mutations, or gene expression levels in order to identify cancer patients that will or are likely to respond to treatment with a histone deacetylase (HDAC) inhibitor, alone or in combination with another cancer treatment. The methods may, optionally, further include treating such patient with an HDAC inhibitor, alone or in combination with another cancer treatment.

公开(公告)号：US20160346279A1

公开(公告)日：2016-12-01

申请号：US15170335

申请日：2016-06-01

申请人： Acetylon Pharmaceuticals, Inc. ,  Board of Regents, The University of Texas System

发明人： Annemieke Kavelaars ,  Cobi J. Heijnen ,  Karen Krukowski ,  Matthew B. Jarpe

IPC分类号： A61K31/505

CPC分类号： A61K31/505 ,  A61K33/24 ,  A61K2300/00

摘要： Disclosed are methods for treating cisplatin-induced peripheral neuropathy in a subject in need thereof comprising administering to the subject a therapeutically effective amount of a histone deacetylase 6 selective inhibitor.

摘要翻译： 公开了在有需要的受试者中治疗顺铂诱导的周围神经病变的方法，包括向受试者施用治疗有效量的组蛋白脱乙酰酶6选择性抑制剂。

公开(公告)号：US09421212B2

公开(公告)日：2016-08-23

申请号：US14824831

申请日：2015-08-12

申请人： Acetylon Pharmaceuticals, Inc.

发明人： John H. van Duzer ,  Ralph Mazitschek

IPC分类号： A61K31/5377 ,  A61K31/4045 ,  A61K31/4709 ,  A61K31/496 ,  A61K31/498 ,  C07D215/48 ,  C07D231/56 ,  C07D333/20 ,  C07D401/12 ,  C07D409/12 ,  C07D471/04 ,  C07D209/08

CPC分类号： C07D409/12 ,  A61K31/4045 ,  A61K31/4709 ,  A61K31/496 ,  A61K31/498 ,  A61K31/5377 ,  C07D209/08 ,  C07D209/34 ,  C07D215/48 ,  C07D215/54 ,  C07D231/56 ,  C07D333/20 ,  C07D401/12 ,  C07D471/04

摘要： Provided herein are compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with HDAC activity, particularly diseases or disorders that involve activity of HDAC1 and/or HDAC2. Such diseases include cancer, sickle-cell anemia, beta-thalassemia, and HIV.

公开(公告)号：US09403779B2

公开(公告)日：2016-08-02

申请号：US14506889

申请日：2014-10-06

申请人： ACETYLON PHARMACEUTICALS, INC.

发明人： David Lee Tamang ,  Min Yang ,  Simon S. Jones

IPC分类号： A61K31/505 ,  C07D239/42 ,  A61K31/517 ,  A61K31/5377

CPC分类号： A61K31/505 ,  A61K31/517 ,  A61K31/519 ,  A61K31/5377 ,  A61K45/06 ,  C07D239/42 ,  A61K2300/00

摘要： The invention relates to combinations comprising an HDAC inhibitor and a Her2 inhibitor for the treatment of breast cancer in a subject in need thereof. The invention also relates to combinations comprising an HDAC inhibitor and a PI3K inhibitor for the treatment of breast cancer in a subject in need thereof. Also provided herein are methods for treating breast cancer in a subject in need thereof comprising administering to the subject an effective amount of one of the above combinations. Further provided are methods for inhibiting migration and/or invasion of a breast cancer cell in a subject by administering to the subject a HDAC6 specific inhibitor.

摘要翻译： 本发明涉及包含HDAC抑制剂和Her2抑制剂的组合物，用于在有需要的受试者中治疗乳腺癌。 本发明还涉及包含HDAC抑制剂和PI3K抑制剂的组合，用于在有需要的受试者中治疗乳腺癌。 本文还提供了在有需要的受试者中治疗乳腺癌的方法，其包括向受试者施用有效量的上述组合之一。 还提供了通过向受试者施用HDAC6特异性抑制剂来抑制受试者中乳腺癌细胞迁移和/或侵袭的方法。

公开(公告)号：US09139583B2

公开(公告)日：2015-09-22

申请号：US14169775

申请日：2014-01-31

申请人： Acetylon Pharmaceuticals, Inc.

发明人： John H. van Duzer ,  Ralph Mazitschek

IPC分类号： C07D471/04 ,  C07D231/56 ,  C07D215/54 ,  C07D209/34 ,  C07D235/06

CPC分类号： C07D471/04 ,  C07D209/34 ,  C07D215/54 ,  C07D231/56 ,  C07D235/06

摘要： Provided herein are inhibitors of HDAC3, as well as methods of treatment comprising administering those compounds to a subject in need thereof.

摘要翻译： 本文提供的是HDAC3的抑制剂，以及治疗方法，包括向有需要的受试者施用这些化合物。

公开(公告)号：US11872227B2

公开(公告)日：2024-01-16

申请号：US17741146

申请日：2022-05-10

申请人： ACETYLON PHARMACEUTICALS, INC.

发明人： Brian North ,  Steven Quayle

IPC分类号： A61K31/505 ,  A61P35/00 ,  A61K31/55

CPC分类号： A61K31/505 ,  A61K31/55 ,  A61P35/00

摘要： The present disclosure relates to a pharmaceutical combination comprising (a) a histone deacetylase 6 inhibitor and (b) an aurora kinase inhibitor, including combined preparations and pharmaceutical compositions thereof; uses of such combination in the treatment or prevention of cancer; and methods of treating or preventing cancer in a subject comprising administering a therapeutically effective amount of such combination.