BR112017012504A2 - derivados de piperidina como inibidores de hdac1/2 - Google Patents
derivados de piperidina como inibidores de hdac1/2Info
- Publication number
- BR112017012504A2 BR112017012504A2 BR112017012504-8A BR112017012504A BR112017012504A2 BR 112017012504 A2 BR112017012504 A2 BR 112017012504A2 BR 112017012504 A BR112017012504 A BR 112017012504A BR 112017012504 A2 BR112017012504 A2 BR 112017012504A2
- Authority
- BR
- Brazil
- Prior art keywords
- hdac1
- inhibitors
- piperidine derivatives
- compounds
- methods
- Prior art date
Links
Classifications
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/496—Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
- A61K31/5375—1,4-Oxazines, e.g. morpholine
- A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
- A61P35/02—Antineoplastic agents specific for leukemia
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P7/00—Drugs for disorders of the blood or the extracellular fluid
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D211/00—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
- C07D211/04—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
- C07D211/06—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
- C07D211/36—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no 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, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
- C07D211/56—Nitrogen atoms
- C07D211/58—Nitrogen atoms attached in position 4
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
- C07D401/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
- C07D409/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
- C07D409/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
- C07D409/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing three or more hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
Abstract
são fornecidos no presente documento compostos, composições farmacêuticas que compreendem tais compostos e métodos de uso de tais compostos para tratar doenças ou distúrbios associados à atividade de hdac1 e/ou hdac2.
Applications Claiming Priority (5)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US201462091221P | 2014-12-12 | 2014-12-12 | |
US62/091,221 | 2014-12-12 | ||
US201562238931P | 2015-10-08 | 2015-10-08 | |
US62/238,931 | 2015-10-08 | ||
PCT/US2015/065289 WO2016094824A1 (en) | 2014-12-12 | 2015-12-11 | Piperidine derivatives as hdac1/2 inhibitors |
Publications (1)
Publication Number | Publication Date |
---|---|
BR112017012504A2 true BR112017012504A2 (pt) | 2018-01-09 |
Family
ID=56108272
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
BR112017012504-8A BR112017012504A2 (pt) | 2014-12-12 | 2015-12-11 | derivados de piperidina como inibidores de hdac1/2 |
Country Status (17)
Country | Link |
---|---|
US (6) | US9790180B2 (pt) |
EP (2) | EP3725787B1 (pt) |
JP (1) | JP6693957B2 (pt) |
KR (1) | KR20170095964A (pt) |
CN (1) | CN107835810A (pt) |
AU (2) | AU2015360270B9 (pt) |
BR (1) | BR112017012504A2 (pt) |
CA (1) | CA2970500C (pt) |
CL (1) | CL2017001511A1 (pt) |
EA (1) | EA035120B1 (pt) |
ES (1) | ES2816641T3 (pt) |
HK (1) | HK1251566A1 (pt) |
IL (1) | IL252828A0 (pt) |
MX (2) | MX2017007623A (pt) |
PH (1) | PH12017501095A1 (pt) |
SG (1) | SG11201704759QA (pt) |
WO (1) | WO2016094824A1 (pt) |
Families Citing this family (12)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
JP2015515279A (ja) | 2012-04-19 | 2015-05-28 | 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. | 治療に反応する患者を同定するバイオマーカーおよびそのような患者の治療 |
US9145412B2 (en) | 2012-11-02 | 2015-09-29 | Acetylon Pharmaceuticals, Inc. | Selective HDAC1 and HDAC2 inhibitors |
US9403779B2 (en) | 2013-10-08 | 2016-08-02 | Acetylon Pharmaceuticals, Inc. | Combinations of histone deacetylase inhibitors and either Her2 inhibitors or PI3K inhibitors |
CA2932411A1 (en) | 2013-12-03 | 2015-06-11 | Acetylon Pharmaceuticals, Inc. | Combinations of histone deacetylase inhibitors and immunomodulatory drugs |
CN107835810A (zh) * | 2014-12-12 | 2018-03-23 | 瑞格纳西制药有限公司 | 作为hdac1/2抑制剂的哌啶衍生物 |
RU2770061C2 (ru) | 2014-12-12 | 2022-04-14 | Джапан Тобакко Инк. | Соединения дигидропиримидин-2-она и их медицинское применение |
AR105812A1 (es) | 2015-06-08 | 2017-11-15 | Acetylon Pharmaceuticals Inc | Métodos para la preparación de inhibidores de proteína deacetilasa |
WO2016200919A1 (en) | 2015-06-08 | 2016-12-15 | Acetylon Pharmaceuticals, Inc. | Crystalline forms of a histone deacetylase inhibitor |
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 |
CA3087994A1 (en) | 2018-02-28 | 2019-09-06 | Japan Tobacco Inc. | 4-methyldihydropyrimidinone compounds and pharmaceutical use thereof |
CN110372572A (zh) * | 2019-08-23 | 2019-10-25 | 苏州汉德创宏生化科技有限公司 | 一种4,4-二氟哌啶-1-甲酰氯的合成方法 |
WO2024030659A1 (en) | 2022-08-05 | 2024-02-08 | Tango Therapeutics, Inc. | An hdac inhibitor for treating cancer with a modified stk11 activity or expression |
Family Cites Families (34)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
OA12790A (en) * | 2002-03-13 | 2006-07-10 | Janssen Pharmaceutica Nv | New inhibitors of histone deacetylase. |
CN101450934B (zh) * | 2002-03-13 | 2012-10-10 | 詹森药业有限公司 | 用作组蛋白去乙酰酶抑制剂的磺酰基衍生物 |
AU2004276337B2 (en) * | 2003-09-24 | 2009-11-12 | Methylgene Inc. | Inhibitors of histone deacetylase |
AR057579A1 (es) * | 2005-11-23 | 2007-12-05 | Merck & Co Inc | Compuestos espirociclicos como inhibidores de histona de acetilasa (hdac) |
AU2007234843B2 (en) * | 2006-04-07 | 2013-07-11 | Methylgene Inc. | Inhibitors of histone deacetylase |
US8119685B2 (en) | 2006-04-26 | 2012-02-21 | Merck Sharp & Dohme Corp. | Disubstituted aniline compounds |
US8119652B2 (en) * | 2006-05-18 | 2012-02-21 | Merck Sharp & Dohme Corp. | Aryl-fused spirocyclic compounds |
EP2174938A1 (en) * | 2006-10-12 | 2010-04-14 | SuperGen, Inc. | Quinoline derivatives for modulating DNA methylation |
JP2010120852A (ja) | 2007-03-09 | 2010-06-03 | Daiichi Sankyo Co Ltd | 新規なジアミド誘導体 |
CN101861151B (zh) | 2007-09-14 | 2014-08-13 | 梅特希尔基因公司 | 使用组蛋白脱乙酰基酶hdac1、hdac2和/或hdac3的选择性抑制剂和微管稳定剂的癌症组合治疗 |
US7790746B2 (en) * | 2007-10-12 | 2010-09-07 | Supergen, Inc. | Quinoline derivatives for modulating DNA methylation |
US7939546B2 (en) * | 2007-10-12 | 2011-05-10 | Supergen, Inc. | Quinoline derivatives for modulating DNA methylation |
EP2526093B1 (en) | 2010-01-22 | 2016-08-17 | Acetylon Pharmaceuticals, Inc. | Reverse amide compounds as protein deacetylase inhibitors and methods of use thereof |
WO2012018499A2 (en) | 2010-08-05 | 2012-02-09 | Acetylon Pharmaceuticals | Specific regulation of cytokine levels by hdac6 inhibitors |
PT2640709T (pt) | 2010-11-16 | 2016-07-13 | Acetylon Pharmaceuticals Inc | Compostos de pirimidina hidroxiamida como inibidores de proteína desacetilase e métodos de utilização dos mesmos |
CA2825599C (en) | 2011-02-01 | 2021-07-13 | The Board Of Trustees Of The University Of Illinois | 4-methyl-n-hydroxybenzamide compounds as histone deacetylase (hdac) inhibitors |
CN102775356B (zh) * | 2011-05-13 | 2015-07-22 | 江苏恒谊药业有限公司 | 4-氨基喹唑啉衍生物及其应用 |
KR20130077390A (ko) * | 2011-12-29 | 2013-07-09 | 제이더블유중외제약 주식회사 | 단백질 키나아제 저해활성을 가지는 6-아미노-3-카복스아미도인다졸 유도체 |
JP2015515279A (ja) | 2012-04-19 | 2015-05-28 | 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. | 治療に反応する患者を同定するバイオマーカーおよびそのような患者の治療 |
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 |
US20140357512A1 (en) | 2013-06-03 | 2014-12-04 | Acetylon Pharmaceuticals, Inc. | Histone deacetylase (hdac) biomarkers in multiple myeloma |
US9403779B2 (en) | 2013-10-08 | 2016-08-02 | Acetylon Pharmaceuticals, Inc. | Combinations of histone deacetylase inhibitors and either Her2 inhibitors or PI3K inhibitors |
EP3054954A4 (en) | 2013-10-10 | 2017-12-13 | Acetylon Pharmaceuticals, Inc. | Hdac inhibitors, alone or in combination with btk inhibitors, for treating non-hodgkin's lymphoma |
ES2818933T3 (es) | 2013-10-10 | 2021-04-14 | Acetylon Pharmaceuticals Inc | Inhibidores de la HDAC en combinación con los inhibidores de la pi3k, para el tratamiento del linfoma no Hodgkin |
WO2015054474A1 (en) | 2013-10-10 | 2015-04-16 | Acetylon Pharmaceuticals, Inc. | Pyrimidine hydroxy amide compounds as histone deacetylase inhibitors |
PE20161342A1 (es) | 2013-10-11 | 2016-12-31 | Acetylon Pharmaceuticals Inc | Combinaciones de inhibidores de histona desacetilasa y farmacos inmunomoduladores |
CA2932411A1 (en) | 2013-12-03 | 2015-06-11 | Acetylon Pharmaceuticals, Inc. | Combinations of histone deacetylase inhibitors and immunomodulatory drugs |
EP3084446B1 (en) | 2013-12-20 | 2022-12-14 | Acetylon Pharmaceuticals, Inc. | Histone deacetylase 6 (hdac6) biomarkers in multiple myeloma |
US9464073B2 (en) | 2014-02-26 | 2016-10-11 | Acetylon Pharmaceuticals, Inc. | Pyrimidine hydroxy amide compounds as HDAC6 selective inhibitors |
CN107205988A (zh) | 2014-07-07 | 2017-09-26 | 埃斯泰隆制药公司 | 利用组蛋白脱乙酰酶抑制剂治疗白血病 |
US20160137630A1 (en) | 2014-10-08 | 2016-05-19 | Acetylon Pharmaceuticals, Inc. | Induction of gata2 by hdac1 and hdac2 inhibitors |
CN107835810A (zh) * | 2014-12-12 | 2018-03-23 | 瑞格纳西制药有限公司 | 作为hdac1/2抑制剂的哌啶衍生物 |
-
2015
- 2015-12-11 CN CN201580076059.1A patent/CN107835810A/zh active Pending
- 2015-12-11 EP EP20160447.7A patent/EP3725787B1/en not_active Withdrawn - After Issue
- 2015-12-11 KR KR1020177019370A patent/KR20170095964A/ko unknown
- 2015-12-11 ES ES15868544T patent/ES2816641T3/es active Active
- 2015-12-11 WO PCT/US2015/065289 patent/WO2016094824A1/en active Application Filing
- 2015-12-11 SG SG11201704759QA patent/SG11201704759QA/en unknown
- 2015-12-11 CA CA2970500A patent/CA2970500C/en active Active
- 2015-12-11 JP JP2017531260A patent/JP6693957B2/ja active Active
- 2015-12-11 MX MX2017007623A patent/MX2017007623A/es active IP Right Grant
- 2015-12-11 AU AU2015360270A patent/AU2015360270B9/en not_active Ceased
- 2015-12-11 EP EP15868544.6A patent/EP3292113B1/en active Active
- 2015-12-11 BR BR112017012504-8A patent/BR112017012504A2/pt not_active Application Discontinuation
- 2015-12-11 US US14/966,556 patent/US9790180B2/en active Active
- 2015-12-11 EA EA201791259A patent/EA035120B1/ru not_active IP Right Cessation
-
2017
- 2017-06-09 MX MX2020002487A patent/MX2020002487A/es unknown
- 2017-06-09 PH PH12017501095A patent/PH12017501095A1/en unknown
- 2017-06-11 IL IL252828A patent/IL252828A0/en unknown
- 2017-06-13 CL CL2017001511A patent/CL2017001511A1/es unknown
- 2017-09-11 US US15/700,998 patent/US10358421B2/en active Active
- 2017-09-29 US US15/719,748 patent/US10239837B2/en active Active
-
2018
- 2018-08-28 HK HK18111028.3A patent/HK1251566A1/zh unknown
-
2019
- 2019-06-06 US US16/433,386 patent/US10968180B2/en active Active
-
2020
- 2020-02-06 AU AU2020200846A patent/AU2020200846A1/en not_active Abandoned
-
2021
- 2021-02-24 US US17/184,118 patent/US11702389B2/en active Active
-
2023
- 2023-05-05 US US18/313,016 patent/US20230348389A1/en active Pending
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Legal Events
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B65X | Notification of requirement for priority examination of patent application | ||
B65Y | Grant of priority examination of the patent application (request complies with dec. 132/06 of 20061117) | ||
B07D | Technical examination (opinion) related to article 229 of industrial property law [chapter 7.4 patent gazette] |
Free format text: DE ACORDO COM O ARTIGO 229-C DA LEI NO 10196/2001, QUE MODIFICOU A LEI NO 9279/96, A CONCESSAO DA PATENTE ESTA CONDICIONADA A ANUENCIA PREVIA DA ANVISA. CONSIDERANDO A APROVACAO DOS TERMOS DO PARECER NO 337/PGF/EA/2010, BEM COMO A PORTARIA INTERMINISTERIAL NO 1065 DE 24/05/2012, ENCAMINHA-SE O PRESENTE PEDIDO PARA AS PROVIDENCIAS CABIVEIS. |
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B07E | Notification of approval relating to section 229 industrial property law [chapter 7.5 patent gazette] |
Free format text: NOTIFICACAO DE ANUENCIA RELACIONADA COM O ART 229 DA LPI |
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B07A | Application suspended after technical examination (opinion) [chapter 7.1 patent gazette] | ||
B07A | Application suspended after technical examination (opinion) [chapter 7.1 patent gazette] | ||
B09B | Patent application refused [chapter 9.2 patent gazette] | ||
B09B | Patent application refused [chapter 9.2 patent gazette] |
Free format text: MANTIDO O INDEFERIMENTO UMA VEZ QUE NAO FOI APRESENTADO RECURSO DENTRO DO PRAZO LEGAL |