JP6816036B2 - ヒストン脱アセチル化阻害剤の結晶形態 - Google Patents

ヒストン脱アセチル化阻害剤の結晶形態 Download PDF

Info

Publication number
JP6816036B2
JP6816036B2 JP2017563542A JP2017563542A JP6816036B2 JP 6816036 B2 JP6816036 B2 JP 6816036B2 JP 2017563542 A JP2017563542 A JP 2017563542A JP 2017563542 A JP2017563542 A JP 2017563542A JP 6816036 B2 JP6816036 B2 JP 6816036B2
Authority
JP
Japan
Prior art keywords
pattern
oxoheptyl
hydroxyamino
carboxamide
chlorophenyl
Prior art date
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Expired - Fee Related
Application number
JP2017563542A
Other languages
English (en)
Japanese (ja)
Other versions
JP2018516946A5 (enExample
JP2018516946A (ja
Inventor
ジョン・エイチ・ヴァン・ドゥーザー
ファルザネー・セイエディ
グイ・リュウ
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Acetylon Pharmaceuticals Inc
Original Assignee
Acetylon Pharmaceuticals Inc
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Acetylon Pharmaceuticals Inc filed Critical Acetylon Pharmaceuticals Inc
Publication of JP2018516946A publication Critical patent/JP2018516946A/ja
Publication of JP2018516946A5 publication Critical patent/JP2018516946A5/ja
Application granted granted Critical
Publication of JP6816036B2 publication Critical patent/JP6816036B2/ja
Expired - Fee Related legal-status Critical Current
Anticipated expiration legal-status Critical

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D239/00Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
    • C07D239/28Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
    • C07D239/32One oxygen, sulfur or nitrogen atom
    • C07D239/42One nitrogen atom
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07BGENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00Indexing scheme relating to specific properties of organic compounds
    • C07B2200/13Crystalline forms, e.g. polymorphs

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Neurology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Biomedical Technology (AREA)
  • Neurosurgery (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
JP2017563542A 2015-06-08 2016-06-08 ヒストン脱アセチル化阻害剤の結晶形態 Expired - Fee Related JP6816036B2 (ja)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201562172629P 2015-06-08 2015-06-08
US62/172,629 2015-06-08
PCT/US2016/036422 WO2016200919A1 (en) 2015-06-08 2016-06-08 Crystalline forms of a histone deacetylase inhibitor

Publications (3)

Publication Number Publication Date
JP2018516946A JP2018516946A (ja) 2018-06-28
JP2018516946A5 JP2018516946A5 (enExample) 2019-07-04
JP6816036B2 true JP6816036B2 (ja) 2021-01-20

Family

ID=56178492

Family Applications (1)

Application Number Title Priority Date Filing Date
JP2017563542A Expired - Fee Related JP6816036B2 (ja) 2015-06-08 2016-06-08 ヒストン脱アセチル化阻害剤の結晶形態

Country Status (6)

Country Link
US (1) US10464906B2 (enExample)
EP (1) EP3303306B1 (enExample)
JP (1) JP6816036B2 (enExample)
AR (1) AR104935A1 (enExample)
TW (1) TW201718516A (enExample)
WO (1) WO2016200919A1 (enExample)

Families Citing this family (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2013158984A1 (en) 2012-04-19 2013-10-24 Acetylon Pharmaceuticals, Inc. Biomarkers to identify patients that will respond to treatment and treating such patients
CA2988594C (en) 2015-06-08 2023-08-15 Acetylon Pharmaceuticals, Inc. Methods of making protein deacetylase inhibitors
EP3468559B1 (en) * 2016-06-09 2023-11-22 Dana Farber Cancer Institute, Inc. Methods of use and pharmaceutical combinations of hdac inhibitors with bet inhibitors
JP7100018B2 (ja) 2016-08-08 2022-07-12 アセチロン ファーマシューティカルズ インコーポレイテッド ヒストンデアセチラーゼ6阻害剤及びcd20阻害抗体の薬学的組み合わせならびにその使用
US11497746B2 (en) 2016-11-23 2022-11-15 Acetylon Pharmaceuticals, Inc. Pharmaceutical combinations comprising a histone deacetylase inhibitor and a programmed death-ligand 1 (PD-L1) inhibitor and methods of use thereof

Family Cites Families (51)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6777217B1 (en) 1996-03-26 2004-08-17 President And Fellows Of Harvard College Histone deacetylases, and uses related thereto
US20030129724A1 (en) 2000-03-03 2003-07-10 Grozinger Christina M. Class II human histone deacetylases, and uses related thereto
WO2001070675A2 (en) 2000-03-24 2001-09-27 Methylgene, Inc. Inhibitors of histone deacetylase
WO2002074298A1 (en) 2001-03-21 2002-09-26 Ono Pharmaceutical Co., Ltd. Il-6 production inhibitors
US7244853B2 (en) 2001-05-09 2007-07-17 President And Fellows Of Harvard College Dioxanes and uses thereof
BR0213791A (pt) 2001-11-01 2004-12-07 Janssen Pharmaceutica Nv Derivados de amida como inibidores de glicogênio sintase quinase 3-beta
US7154002B1 (en) 2002-10-08 2006-12-26 Takeda San Diego, Inc. Histone deacetylase inhibitors
US7381825B2 (en) 2003-03-17 2008-06-03 Takeda San Diego, Inc. Histone deacetylase inhibitors
US8227636B2 (en) 2004-04-05 2012-07-24 Merck Hdac Research, Llc Histone deacetylase inhibitor prodrugs
CN101495116A (zh) 2005-03-22 2009-07-29 哈佛大学校长及研究员协会 蛋白降解病症的治疗
EP1940805A4 (en) 2005-08-26 2009-11-11 Methylgene Inc BENZODIAZEPIN AND BENZOPIPERAZINANALOGA AS INHIBITORS OF HISTONDEACETYLASE
JP5441416B2 (ja) 2006-02-14 2014-03-12 プレジデント アンド フェロウズ オブ ハーバード カレッジ 二官能性ヒストンデアセチラーゼインヒビター
CN101484156B (zh) 2006-05-03 2015-11-25 哈佛大学校长及研究员协会 组蛋白脱乙酰基酶和微管蛋白脱乙酰基酶抑制剂
WO2007144341A1 (en) 2006-06-12 2007-12-21 Vrije Universiteit Brussel Differentiation of rat liver epithelial cells into hepatocyte-like cells
ES2288802B1 (es) 2006-07-07 2008-12-16 Universidad De Granada Nuevos derivados de ftalimida como inhibidores de las histonas desacetilasas.
WO2008033746A2 (en) 2006-09-11 2008-03-20 Curis, Inc. Tyrosine kinase inhibitors containing a zinc binding moiety
EP2255818B1 (en) 2008-02-19 2018-08-22 Earnest Medicine Co., Ltd. Oral or enteral composition useful for recovery of physical functions
RU2515611C2 (ru) 2008-07-23 2014-05-20 Президент Энд Феллоуз Оф Гарвард Колледж Ингибиторы деацетилазы и их применение
WO2010131922A2 (en) 2009-05-15 2010-11-18 Korea Research Institute Of Chemical Technology Amide compound, preparation method thereof and pharmaceutical composition comprising same
US8716344B2 (en) 2009-08-11 2014-05-06 President And Fellows Of Harvard College Class- and isoform-specific HDAC inhibitors and uses thereof
US20130040998A1 (en) 2010-01-08 2013-02-14 Dana-Farber Cancer Institute, Inc. Fluorinated hdac inhibitors and uses thereof
CN102933558B (zh) 2010-01-22 2016-03-16 埃斯泰隆制药公司 作为蛋白质去乙酰化酶抑制剂的反向酰胺化合物及其使用方法
AU2011255281A1 (en) 2010-05-21 2013-01-10 Sloan-Kettering Institute For Cancer Research Selective HDAC inhibitors
WO2012018499A2 (en) 2010-08-05 2012-02-09 Acetylon Pharmaceuticals Specific regulation of cytokine levels by hdac6 inhibitors
NZ710405A (en) 2010-11-16 2017-04-28 Acetylon Pharmaceuticals Inc Pyrimidine hydroxy amide compounds as protein deacetylase inhibitors and methods of use thereof
EP2734500A4 (en) 2011-07-20 2015-04-08 Gen Hospital Corp SELECTIVE HISTONDEACETYLASE-6 INHIBITORS FOR THE TREATMENT OF BONE DISORDERS
WO2013158984A1 (en) 2012-04-19 2013-10-24 Acetylon Pharmaceuticals, Inc. Biomarkers to identify patients that will respond to treatment and treating such patients
HK1213471A1 (zh) 2012-10-12 2016-07-08 The Trustees Of The University Of Pennsylvania 作為蛋白脫乙酰基酶抑制劑的嘧啶羥基酰胺化合物及其使用方法
US9145412B2 (en) 2012-11-02 2015-09-29 Acetylon Pharmaceuticals, Inc. Selective HDAC1 and HDAC2 inhibitors
JP2016511237A (ja) 2013-02-01 2016-04-14 アセチロン ファーマシューティカルズ インコーポレイテッドAcetylon Pharmaceuticals,Inc. 選択的hdac3阻害剤
US9139583B2 (en) 2013-02-01 2015-09-22 Acetylon Pharmaceuticals, Inc. Selective HDAC3 inhibitors
WO2014197471A1 (en) 2013-06-03 2014-12-11 Acetylon Pharmaceuticals, Inc. Histone deacetylase ( hdac) biomarkers in multiple myeloma
JP2016531163A (ja) 2013-09-20 2016-10-06 アセチロン ファーマシューティカルズ インコーポレイテッドAcetylon Pharmaceuticals,Inc. Hdac6阻害物質を用いた、異常なリンパ球の機能に起因する疾患の治療
ES2929576T3 (es) 2013-10-08 2022-11-30 Acetylon Pharmaceuticals Inc Combinaciones de inhibidores de histona deacetilasa 6 y el inhibidor de Her2 lapatinib para el uso en el tratamiento del cáncer de mama
JP2016536354A (ja) 2013-10-10 2016-11-24 アセチロン ファーマシューティカルズ インコーポレイテッドAcetylon Pharmaceuticals,Inc. 非ホジキンリンパ腫を治療するための、hdac阻害剤単独またはbtk阻害剤との組み合わせ
EP3055299B1 (en) 2013-10-10 2021-01-06 Acetylon Pharmaceuticals, Inc. Pyrimidine hydroxy amide compounds as histone deacetylase inhibitors
EP3054953B1 (en) 2013-10-10 2020-07-01 Acetylon Pharmaceuticals, Inc. Hdac inhibitors in combination with pi3k inhibitors, for treating non-hodgkin's lymphoma
EP3054939A4 (en) 2013-10-11 2017-12-13 Acetylon Pharmaceuticals, Inc. Combinations of histone deactylase inhibitors and immunomodulatory drugs
US10660890B2 (en) 2013-10-24 2020-05-26 National Institutes Of Health (Nih), U.S. Dept. Of Health And Human Services (Dhhs), U.S. Government Nih Division Of Extramural Inventions And Technology Resources (Deitr) Treatment of polycystic diseases with an HDAC6 inhibitor
KR20160092018A (ko) 2013-12-03 2016-08-03 에이스틸론 파마수티컬스 인코포레이티드 히스톤 탈아세틸화효소 저해제 및 면역조절 약물의 조합
JP7017309B2 (ja) 2013-12-20 2022-02-08 アセチロン ファーマシューティカルズ インコーポレイテッド 多発性骨髄腫におけるヒストン脱アセチル化酵素6(hdac6)バイオマーカー
US9464073B2 (en) 2014-02-26 2016-10-11 Acetylon Pharmaceuticals, Inc. Pyrimidine hydroxy amide compounds as HDAC6 selective inhibitors
US20150359794A1 (en) 2014-06-13 2015-12-17 Buck Institute For Research On Aging Impairment of the large ribosomal subunit protein rpl24 by depletion or acetylation
AU2015288060A1 (en) 2014-07-07 2017-02-09 Acetylon Pharmaceuticals, Inc. Treatment of leukemia with histone deacetylase inhibitors
EP3204006A4 (en) 2014-10-08 2018-04-04 Regenacy Pharmaceuticals, LLC Induction of gata2 by hdac1 and hdac2 inhibitors
WO2016090230A1 (en) 2014-12-05 2016-06-09 Acetylon Pharmaceuticals, Inc. Pyrimidine hydroxy amide compounds for treating peripheral neuropathy
AU2015356779A1 (en) 2014-12-05 2017-07-13 University of Modena and Reggio Emilia Combinations of histone deacetylase inhibitors and bendamustine for use in the treatment of lymphoma
US9790180B2 (en) 2014-12-12 2017-10-17 Regenacy Pharmaceuticals, Llc Piperidine derivatives as HDAC1/2 inhibitors
US20160339022A1 (en) 2015-04-17 2016-11-24 Acetylon Pharmaceuticals Inc. Treatment of neuroblastoma with histone deacetylase inhibitors
US10272084B2 (en) 2015-06-01 2019-04-30 Regenacy Pharmaceuticals, Llc Histone deacetylase 6 selective inhibitors for the treatment of cisplatin-induced peripheral neuropathy
CA2988594C (en) 2015-06-08 2023-08-15 Acetylon Pharmaceuticals, Inc. Methods of making protein deacetylase inhibitors

Also Published As

Publication number Publication date
AR104935A1 (es) 2017-08-23
EP3303306B1 (en) 2020-02-12
WO2016200919A1 (en) 2016-12-15
US10464906B2 (en) 2019-11-05
TW201718516A (zh) 2017-06-01
US20170001965A1 (en) 2017-01-05
JP2018516946A (ja) 2018-06-28
EP3303306A1 (en) 2018-04-11

Similar Documents

Publication Publication Date Title
CN105209437B (zh) 心肌肌球蛋白激动剂的盐和制备盐的方法
TWI882617B (zh) 3-((1r,3r)-1-(2,6-二氟-4-((1-(3-氟丙基)氮雜環丁-3-基)胺基)苯基)-3-甲基-1,3,4,9-四氫-2h-吡啶并[3,4-b]吲哚-2-基)-2,2-二氟丙-1-醇之固體形式及用於製備包含經取代苯基或吡啶基部分之稠合三環化合物之製程,包括其使用方法
JP6816036B2 (ja) ヒストン脱アセチル化阻害剤の結晶形態
JP2018520205A (ja) レンバチニブメシル酸塩の新規結晶形及びその製造方法
CN110650963A (zh) (S)-2-((2-((S)-4-(二氟甲基)-2-氧代噁唑烷-3-基)-5,6-二氢苯并[f]咪唑并[1,2-d][1,4]氧氮杂*-9-基)氨基)丙酰胺的多晶型物和固体形式及其制备方法
WO2011033307A1 (en) Nilotinib dihydrochloride salt
BR112019021447A2 (pt) sal fumarato, forma cristalina i do referido sal, métodos para preparação dos mesmos, composição farmacêutica compreendendo o sal e a forma cristalina i e uso do sal fumarato, da forma cristalina i e da composição farmacêutica
GB2558514A (en) Process for the synthesis of stable amorphous ibrutinib
WO2011023146A1 (en) Imatinib mesylate polymorphs generated by crystallization in aqueous inorganic salt solutions
US9453011B2 (en) Crystal form of dabrafenib mesylate and preparation method thereof
CN105517992A (zh) 新型结晶性芳烷基胺化合物及其制造方法
JP7152122B2 (ja) エダラボン塩
US20220002302A1 (en) Novel polymorphs of acalabrutinib, a bruton's tyrosine kinase inhibitor
CN113840605B (zh) N-(5-((4-乙基哌嗪-1-基)甲基)吡啶-2-基)-5-氟-4-(3-异丙基-2-甲基-2h-吲唑-5-基)嘧啶-2-胺盐酸盐的结晶形式及其用途
CN111499627A (zh) 取代的咪唑并吡啶基-氨基吡啶化合物的盐和多晶型
CN103819461B (zh) N-[3-氯-4-(3-氟苄氧基)苯基]-6-[5-[[2-(甲亚磺酰基)乙基]氨基]甲基]-2-呋喃基]-4-喹唑啉胺多晶型物及其制备方法
CN113149998B (zh) 2-吲哚啉螺环酮类化合物或其盐、溶剂合物的无定形形式或结晶形式
JP2020535192A (ja) レナリドミドの結晶形
KR20200024302A (ko) 페닐 피리미돈 화합물의 염, 다형체 및 이의 약학 조성물 및 용도
HU231012B1 (hu) Lapatinib sók
WO2016081538A1 (en) Solid state forms of ceritinib and salts thereof
WO2022199707A1 (zh) 哌马色林药用盐、制备方法、含其的药物组合物及应用
EP1768969B1 (en) Crystalline mycophenolate sodium
HK40061853B (zh) 用作cdk7激酶抑制剂的化合物及其应用
HK1219484B (zh) 心肌肌球蛋白激动剂的盐和制备盐的方法

Legal Events

Date Code Title Description
A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20190527

A621 Written request for application examination

Free format text: JAPANESE INTERMEDIATE CODE: A621

Effective date: 20190527

A977 Report on retrieval

Free format text: JAPANESE INTERMEDIATE CODE: A971007

Effective date: 20200220

A131 Notification of reasons for refusal

Free format text: JAPANESE INTERMEDIATE CODE: A131

Effective date: 20200309

A601 Written request for extension of time

Free format text: JAPANESE INTERMEDIATE CODE: A601

Effective date: 20200608

A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20200904

TRDD Decision of grant or rejection written
A01 Written decision to grant a patent or to grant a registration (utility model)

Free format text: JAPANESE INTERMEDIATE CODE: A01

Effective date: 20201124

A61 First payment of annual fees (during grant procedure)

Free format text: JAPANESE INTERMEDIATE CODE: A61

Effective date: 20201223

R150 Certificate of patent or registration of utility model

Ref document number: 6816036

Country of ref document: JP

Free format text: JAPANESE INTERMEDIATE CODE: R150

R250 Receipt of annual fees

Free format text: JAPANESE INTERMEDIATE CODE: R250

LAPS Cancellation because of no payment of annual fees