公开(公告)号：US20150045367A1

公开(公告)日：2015-02-12

申请号：US14368475

申请日：2012-12-19

Applicant: PHARMACYCLICS, INC.

Inventor： Erik Verner ,  Wei Chen ,  Sriram Balasubramanian

IPC: C07D405/06 ,  C07D213/89 ,  C07D211/46 ,  C07D295/088 ,  C07D211/42 ,  C07D213/82 ,  C07C235/38 ,  C07C311/08 ,  C07C235/34 ,  C07D401/06

CPC classification number: C07D405/06 ,  C07C235/34 ,  C07C235/38 ,  C07C259/06 ,  C07C311/08 ,  C07D211/42 ,  C07D211/46 ,  C07D213/30 ,  C07D213/36 ,  C07D213/65 ,  C07D213/68 ,  C07D213/82 ,  C07D213/89 ,  C07D295/088 ,  C07D401/06

Abstract: Described herein are compounds and pharmaceutical compositions containing such compounds, which inhibit the activity of histone deacetylase 8 (HDAC8). Also described herein are methods of using such HDAC8 inhibitors, alone and in combination with other compounds, for treating diseases or conditions that would benefit from inhibition of HDAC8 activity.

Abstract translation: 本文描述了含有这种化合物的化合物和药物组合物，其抑制组蛋白脱乙酰酶8（HDAC8）的活性。 本文还描述了将这样的HDAC8抑制剂单独使用并与其它化合物联合用于治疗将受益于抑制HDAC8活性的疾病或病症的方法。

公开(公告)号：US20150164854A1

公开(公告)日：2015-06-18

申请号：US14620075

申请日：2015-02-11

Applicant: Pharmacyclics, Inc.

Inventor： David J. LOURY ,  Joseph J. BUGGY ,  Tarak D. MODY ,  Erik J. VERNER ,  Norbert PURRO ,  Sriram Balasubramanian

IPC: A61K31/343 ,  A61K45/06 ,  A61N5/10 ,  A61K38/05

CPC classification number: A61N5/10 ,  A61K9/205 ,  A61K9/2054 ,  A61K9/2826 ,  A61K9/2846 ,  A61K9/2866 ,  A61K9/4808 ,  A61K9/4858 ,  A61K9/4866 ,  A61K9/501 ,  A61K9/5026 ,  A61K31/166 ,  A61K31/343 ,  A61K31/35 ,  A61K31/381 ,  A61K31/40 ,  A61K31/4184 ,  A61K31/47 ,  A61K31/497 ,  A61K31/573 ,  A61K31/69 ,  A61K31/704 ,  A61K38/05 ,  A61K45/05 ,  A61K45/06 ,  A61K47/02 ,  A61K47/12 ,  C07D307/85

Abstract: Dosing regimens, methods of treatment, controlled release formulations, and combination therapies that include an HDAC inhibitor, or a pharmaceutically acceptable salt thereof, are described.

Abstract translation: 描述了给药方案，治疗方法，控制释放制剂和包括HDAC抑制剂或其药学上可接受的盐的组合疗法。

公开(公告)号：US08906954B2

公开(公告)日：2014-12-09

申请号：US13897582

申请日：2013-05-20

Applicant: Pharmacyclics, Inc.

Inventor： Erik Verner ,  Sriram Balasubramanian ,  Joseph J. Buggy

IPC: A61K31/40

CPC classification number: A61K45/06 ,  A61K31/40 ,  A61K31/404 ,  A61K31/4439 ,  A61K31/5377 ,  C07D207/337 ,  C07D209/08 ,  C07D209/12 ,  C07D209/14 ,  C07D235/06 ,  C07D307/79 ,  C07D307/80 ,  C07D333/54 ,  C07D333/56 ,  C07D401/06 ,  C07D401/12 ,  C07D405/06 ,  C07D409/06 ,  C07D471/04 ,  Y02A50/40

Abstract: Described herein are compounds and pharmaceutical compositions containing such compounds, which inhibit the activity of histone deacetylase 8 (HDAC8). Also described herein are methods of using such HDAC8 inhibitors, alone and in combination with other compounds, for treating diseases or conditions that would benefit from inhibition of HDAC8 activity.

Abstract translation: 本文描述了含有这种化合物的化合物和药物组合物，其抑制组蛋白脱乙酰酶8（HDAC8）的活性。 本文还描述了将这样的HDAC8抑制剂单独使用并与其它化合物联合用于治疗将受益于抑制HDAC8活性的疾病或病症的方法。

公开(公告)号：US20150024040A1

公开(公告)日：2015-01-22

申请号：US14510369

申请日：2014-10-09

Applicant: LES LABORATORIES SERVIER ,  PHARMACYCLICS, INC.

Inventor： Ioana Kloos ,  Renata Robert ,  Anne Jacquet-Bescond ,  Stéphane Depil ,  Marylore Chenel ,  Sylvain Fouliard ,  Sriram Balasubramanian

IPC: A61K31/343 ,  A61N5/10 ,  A61K31/138 ,  A61K33/24 ,  A61K31/704

CPC classification number: A61K31/343 ,  A61K31/138 ,  A61K31/704 ,  A61K33/24 ,  A61N5/10 ,  A61K2300/00

Abstract: N-hydroxy-4-{2-[3-(N,N-dimethylaminomethyl)benzofuran-2-ylcarbonylamino]ethoxy}-benzamide of formula (I): or an addition salt thereof with a pharmaceutically acceptable acid or base, alone or in association with surgery, chemotherapy or hormone therapy treatment or radiotherapy, for use in the treatment of cancer, characterised in that it is administered for 4 consecutive days, that period being followed by 3 consecutive days without any administration of compound of formula (I), with the proviso that the chemotherapy is not FOLFOX.

Abstract translation: 式（I）的N-羟基-4- {2- [3-（N，N-二甲基氨基甲基）苯并呋喃-2-基羰基氨基]乙氧基} - 苯甲酰胺或其药学上可接受的酸或碱的加成盐，单独或 与用于治疗癌症的手术，化学疗法或激素疗法治疗或放射疗法联合使用，其特征在于其连续连续服用4天，随后连续3天，而不施用式（I）化合物， ，但条件是化疗不是FOLFOX。

公开(公告)号：US08900565B2

公开(公告)日：2014-12-02

申请号：US13683880

申请日：2012-11-21

Applicant: Pharmacyclics, Inc.

Inventor： Joseph J. Buggy ,  Sriram Balasubramanian ,  Erik Verner ,  Vincent W. F. Tai ,  Chang-Sun Lee

IPC: A61K31/405 ,  A61K31/55 ,  A61K45/06 ,  C07D209/08 ,  C07D209/42 ,  A61K31/5377 ,  C07D209/12 ,  A61K31/404 ,  C07D209/14

CPC classification number: C07D209/08 ,  A61K31/404 ,  A61K31/5377 ,  A61K45/06 ,  C07D209/12 ,  C07D209/14 ,  C07D209/42 ,  C07D403/06 ,  A61K2300/00 ,  A61K31/55

Abstract: Described herein are compounds and pharmaceutical compositions containing such compounds, which inhibit the activity of histone deacetylase 8 (HDAC8). Also described herein are methods of using such HDAC8 inhibitors, alone and in combination with other compounds, for treating diseases or conditions that would benefit from inhibition of HDAC8 activity.

Abstract translation: 本文描述了含有这种化合物的化合物和药物组合物，其抑制组蛋白脱乙酰酶8（HDAC8）的活性。 本文还描述了将这样的HDAC8抑制剂单独使用并与其它化合物联合用于治疗将受益于抑制HDAC8活性的疾病或病症的方法。

公开(公告)号：US20130156727A1

公开(公告)日：2013-06-20

申请号：US13683880

申请日：2012-11-21

Applicant: Pharmacyclics, Inc.

Inventor： Joseph J. BUGGY ,  Sriram Balasubramanian ,  Erik Verner ,  Vincent W.F. Tai ,  Chang-Sun Lee

IPC: A61K45/06 ,  A61K31/404 ,  A61K31/5377 ,  C07D209/42

CPC classification number: C07D209/08 ,  A61K31/404 ,  A61K31/5377 ,  A61K45/06 ,  C07D209/12 ,  C07D209/14 ,  C07D209/42 ,  C07D403/06 ,  A61K2300/00 ,  A61K31/55

Abstract: Described herein are compounds and pharmaceutical compositions containing such compounds, which inhibit the activity of histone deacetylase 8 (HDAC8). Also described herein are methods of using such HDAC8 inhibitors, alone and in combination with other compounds, for treating diseases or conditions that would benefit from inhibition of HDAC8 activity.

公开(公告)号：US20130078215A1

公开(公告)日：2013-03-28

申请号：US13668170

申请日：2012-11-02

Applicant: PHARMACYCLICS, INC.

Inventor： Joseph J. Buggy ,  Sriram Balasubramanian ,  Susanne M. Steggerda

IPC: C07D209/10 ,  C07D403/06 ,  C07D209/08 ,  C07D209/12 ,  A61K45/06 ,  A61K31/405 ,  A61K31/454 ,  A61K31/5377 ,  A61K31/4245 ,  C07D401/06 ,  C07D413/06

CPC classification number: C07D209/12 ,  A61K31/404 ,  A61K31/4045 ,  A61K31/405 ,  A61K31/4245 ,  A61K31/454 ,  A61K31/5377 ,  A61K45/06 ,  C07D209/08 ,  C07D209/10 ,  C07D401/06 ,  C07D403/06 ,  C07D413/06

Abstract: Described herein are methods for treating a subject suffering from an inflammatory, autoimmune, or heteroimmune condition by administering to the subject a pharmaceutical composition containing a therapeutically effective amount of a compound that is a selective inhibitor of histone deacetylase 8. Also described herein are methods for decreasing secretion of pro-inflammatory cytokines by administering an HDAC8-selective inhibitor compound. Further described herein are methods for predicting responsiveness to treatments for inflammatory conditions. Methods for predicting efficacy of treatments for inflammatory conditions are also described.

Abstract translation: 本文描述了通过向受试者施用含有治疗有效量的作为组蛋白脱乙酰酶8的选择性抑制剂的化合物的药物组合物来治疗患有炎症，自身免疫或异种免疫病症的受试者的方法。本文还描述了用于 通过施用HDAC8选择性抑制剂化合物来减少促炎细胞因子的分泌。 本文进一步描述了用于预测对治疗炎症反应的方法。 还描述了用于预测炎症病症治疗功效的方法。

公开(公告)号：US20150038513A1

公开(公告)日：2015-02-05

申请号：US14130134

申请日：2012-07-03

Applicant: LES LABORATOIRES SERVIER ,  PHARMACYCLICS, INC.

Inventor： Stéphane Depil ,  Anne Jacquet-Bescond ,  Ioana Kloos ,  Anne-Laure Sarry ,  Sriram Balasubramanian ,  Joseph Buggy

IPC: A61K31/343 ,  A61K31/513 ,  A61K31/282 ,  A61K31/519

CPC classification number: A61K31/343 ,  A61K31/19 ,  A61K31/282 ,  A61K31/505 ,  A61K31/513 ,  A61K31/519 ,  C07D307/85 ,  C07D333/70 ,  C07D405/06 ,  C07D405/12 ,  A61K31/424

Abstract: Association between N-hydroxy-4-{2-[3-(N,N-dimethylaminomethyl)benzofuran-2-yl-carbonylamino]ethoxy}benzamide of formula (I): an addition salt thereof with a pharmaceutically acceptable acid or base, and FOLFOX.Medicaments.

Abstract translation: 式（I）的N-羟基-4- {2- [3-（N，N-二甲基氨基甲基）苯并呋喃-2-基 - 羰基氨基]乙氧基}苯甲酰胺与其药学上可接受的酸或碱的加成盐， 和FOLFOX。 药剂

公开(公告)号：US20140057862A1

公开(公告)日：2014-02-27

申请号：US14069233

申请日：2013-10-31

Applicant: Pharmacyclics, Inc.

Inventor： David J. LOURY ,  Joseph J. BUGGY ,  Tarak D. MODY ,  Erik J. VERNER ,  Norbert PURRO ,  Sriram Balasubramanian

IPC: A61K31/343 ,  A61K45/06 ,  A61K31/704 ,  A61K31/573 ,  C07D307/85 ,  A61K31/4184

CPC classification number: A61N5/10 ,  A61K9/205 ,  A61K9/2054 ,  A61K9/2826 ,  A61K9/2846 ,  A61K9/2866 ,  A61K9/4808 ,  A61K9/4858 ,  A61K9/4866 ,  A61K9/501 ,  A61K9/5026 ,  A61K31/166 ,  A61K31/343 ,  A61K31/35 ,  A61K31/381 ,  A61K31/40 ,  A61K31/4184 ,  A61K31/47 ,  A61K31/497 ,  A61K31/573 ,  A61K31/69 ,  A61K31/704 ,  A61K38/05 ,  A61K45/05 ,  A61K45/06 ,  A61K47/02 ,  A61K47/12 ,  C07D307/85

Abstract: Dosing regimens, methods of treatment, controlled release formulations, and combination therapies that include an HDAC inhibitor, or a pharmaceutically acceptable salt thereof, are described.

Abstract translation: 描述了给药方案，治疗方法，控制释放制剂和包括HDAC抑制剂或其药学上可接受的盐的组合疗法。