CL2016003301A1 - Compuestos derivados del ácido amino-(piridin-4-carboxílico) sustituidos, inhibidores de la histona desmetilasa; composición farmacéutica, que los comprende, útiles en el tratamiento del cáncer, tales como el cáncer de próstata, mama, vejiga, pulmón y/o melanoma. - Google Patents

Compuestos derivados del ácido amino-(piridin-4-carboxílico) sustituidos, inhibidores de la histona desmetilasa; composición farmacéutica, que los comprende, útiles en el tratamiento del cáncer, tales como el cáncer de próstata, mama, vejiga, pulmón y/o melanoma.

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Publication number
CL2016003301A1
CL2016003301A1 CL2016003301A CL2016003301A CL2016003301A1 CL 2016003301 A1 CL2016003301 A1 CL 2016003301A1 CL 2016003301 A CL2016003301 A CL 2016003301A CL 2016003301 A CL2016003301 A CL 2016003301A CL 2016003301 A1 CL2016003301 A1 CL 2016003301A1
Authority
CL
Chile
Prior art keywords
cancer
prostate
bladder
breast
lung
Prior art date
Application number
CL2016003301A
Other languages
English (en)
Inventor
Amogh Boloor
Young K Chen
Michael Brennan Wallace
Original Assignee
Celgene Quanticel Res 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 Celgene Quanticel Res Inc filed Critical Celgene Quanticel Res Inc
Publication of CL2016003301A1 publication Critical patent/CL2016003301A1/es

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
    • C07D405/12—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
    • 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
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • 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
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/4433—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with oxygen as a ring hetero atom
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom 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
    • C07D213/78—Carbon atoms having three bonds to hetero atoms, with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C07D213/79—Acids; Esters
    • 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
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/14—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero 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
    • C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen 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
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a chain containing hetero atoms as chain links

Abstract

La presente invención se refiere a un compuesto, o un estereoisómero o sal farmacéuticamente aceptable del mismo, que tiene la estructura de la fórmula (II): Además, la invención divulga el compuesto, o sal farmacéuticamente aceptable del mismo, de la reivindicación 1 de fórmula (IIa): Además, la presente invención divulga un método in vitro para inhibir una enzima JMJD3 de histona desmetilasa que comprende poner en contacto la enzima histona desmetilasa JMJD3 con un compuesto de fórmula (II), la presente invención divulga el uso del compuesto de fórmula (II).
CL2016003301A 2014-06-25 2016-12-22 Compuestos derivados del ácido amino-(piridin-4-carboxílico) sustituidos, inhibidores de la histona desmetilasa; composición farmacéutica, que los comprende, útiles en el tratamiento del cáncer, tales como el cáncer de próstata, mama, vejiga, pulmón y/o melanoma. CL2016003301A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US201462017201P 2014-06-25 2014-06-25

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CL2016003301A1 true CL2016003301A1 (es) 2021-03-05

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CL2016003301A CL2016003301A1 (es) 2014-06-25 2016-12-22 Compuestos derivados del ácido amino-(piridin-4-carboxílico) sustituidos, inhibidores de la histona desmetilasa; composición farmacéutica, que los comprende, útiles en el tratamiento del cáncer, tales como el cáncer de próstata, mama, vejiga, pulmón y/o melanoma.

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US (7) US10385047B2 (es)
EP (3) EP3160952B1 (es)
JP (1) JP6521535B2 (es)
KR (1) KR102591897B1 (es)
CN (2) CN111909083B (es)
AR (1) AR100997A1 (es)
AU (1) AU2015279719B2 (es)
BR (1) BR112016030367A2 (es)
CA (1) CA2953437C (es)
CL (1) CL2016003301A1 (es)
CO (1) CO2017000359A2 (es)
CY (1) CY1123906T1 (es)
DK (1) DK3160952T3 (es)
EA (1) EA031200B1 (es)
EC (1) ECSP17004931A (es)
ES (1) ES2862648T3 (es)
HR (1) HRP20210299T1 (es)
HU (1) HUE053876T2 (es)
IL (1) IL249629A0 (es)
LT (1) LT3160952T (es)
MX (1) MX2016017407A (es)
NZ (1) NZ728120A (es)
PL (1) PL3160952T3 (es)
PT (1) PT3160952T (es)
SA (1) SA516380585B1 (es)
SG (1) SG11201610813TA (es)
SI (1) SI3160952T1 (es)
TW (2) TWI715533B (es)
WO (1) WO2015200709A1 (es)

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AU2015279719B2 (en) 2014-06-25 2019-03-21 Celgene Quanticel Research, Inc. Histone demethylase inhibitors
US10030017B2 (en) 2014-09-17 2018-07-24 Celgene Quanticel Research, Inc. Histone demethylase inhibitors
EA201790603A1 (ru) 2014-09-17 2017-10-31 Селджен Квонтисел Рисёрч, Инк. Ингибиторы гистондеметилазы
JP6883913B2 (ja) 2015-12-28 2021-06-09 セルジーン クオンティセル リサーチ，インク． ヒストンデメチラーゼ阻害剤
WO2017161012A1 (en) * 2016-03-15 2017-09-21 Celgene Quanticel Research, Inc. Histone demethylase inhibitors
US10150754B2 (en) 2016-04-19 2018-12-11 Celgene Quanticel Research, Inc. Histone demethylase inhibitors
EP3600301A4 (en) * 2017-03-30 2020-08-12 Albert-Ludwigs-Universität Freiburg KDM4 INHIBITORS
CN109825551B (zh) * 2019-02-21 2022-08-02 深圳大学 一种评价组蛋白赖氨酸去甲基转移酶活性的方法
CN111679072B (zh) * 2020-06-15 2022-04-29 温州医科大学 Kdm6b蛋白在乳腺癌预后评估试剂盒、诊断试剂盒中的应用
EP4319748A1 (en) * 2021-04-09 2024-02-14 Tachyon Therapeutics, Inc. Treatment of cancer with kdm4 inhibitors
WO2023023112A1 (en) * 2021-08-18 2023-02-23 Celgene Corporation Process for preparing histone demethylase inhibitors
WO2023122221A1 (en) * 2021-12-23 2023-06-29 Tachyon Therapeutics, Inc. Pharmaceutical formulations comprising 3-({[(4r)-7-{methyl[4-(propan-2-yl)phenyl]amino}-3,4-dihydro-2h-l-benzopyran-4-yl]methyl}amino)pyridine-4-carboxylic acid
WO2023250480A1 (en) * 2022-06-23 2023-12-28 The Cleveland Clinic Foundation 3-βHSD1 INHIBITORS AND COMPOSITIONS AND USES THEREOF
WO2024064734A1 (en) * 2022-09-21 2024-03-28 Celgene Corporation Crystalline forms of 3-({[(4r)-7-{methyl[4-(propan-2- yl)phenyl]amino}-3,4-dihydro-2h-l-benzopyran-4- yl]methyl}amino)pyridine-4-carboxylic acid l-lysine salt, a histone demethylase inhibitor
CN115974647A (zh) * 2022-12-05 2023-04-18 江苏宏邦化工科技有限公司 以四氢-4-甲基-2-苯基-2h-吡喃-4-醇为原料制备苯乐戊醇的方法

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EP3160952A4 (en) 2018-02-21
MX2016017407A (es) 2017-04-27
SA516380585B1 (ar) 2020-12-06
US20180044334A1 (en) 2018-02-15
US9586902B2 (en) 2017-03-07
CN111909083B (zh) 2023-08-15
EP3160952A1 (en) 2017-05-03
US10385047B2 (en) 2019-08-20
BR112016030367A2 (pt) 2018-07-17
KR102591897B1 (ko) 2023-10-19
EA031200B1 (ru) 2018-11-30
HUE053876T2 (hu) 2021-07-28
LT3160952T (lt) 2021-05-10
CN111909083A (zh) 2020-11-10
PT3160952T (pt) 2021-03-08
EA201692483A1 (ru) 2017-05-31
TWI758004B (zh) 2022-03-11
JP2017523152A (ja) 2017-08-17
CA2953437C (en) 2022-08-30
US20180251458A1 (en) 2018-09-06
US20170114055A1 (en) 2017-04-27
HRP20210299T1 (hr) 2021-04-16
US9994561B2 (en) 2018-06-12
CY1123906T1 (el) 2022-05-27
US20150376169A1 (en) 2015-12-31
PL3160952T3 (pl) 2021-07-19
EP3741749A1 (en) 2020-11-25
US9447046B2 (en) 2016-09-20
SI3160952T1 (sl) 2021-07-30
US20170158685A1 (en) 2017-06-08
ECSP17004931A (es) 2017-03-31
US20160107995A1 (en) 2016-04-21
JP6521535B2 (ja) 2019-05-29
US9242968B2 (en) 2016-01-26
TW201613882A (en) 2016-04-16
EP3738960A1 (en) 2020-11-18
US10106534B2 (en) 2018-10-23
TWI715533B (zh) 2021-01-11
IL249629A0 (en) 2017-02-28
ES2862648T3 (es) 2021-10-07
KR20170018079A (ko) 2017-02-15
DK3160952T3 (da) 2021-03-08
AU2015279719B2 (en) 2019-03-21
AR100997A1 (es) 2016-11-16
NZ728120A (en) 2023-06-30
US20160332970A1 (en) 2016-11-17
CN106660982A (zh) 2017-05-10
CN106660982B (zh) 2020-09-08
TW202124369A (zh) 2021-07-01
WO2015200709A1 (en) 2015-12-30
CO2017000359A2 (es) 2017-04-10
CA2953437A1 (en) 2015-12-30
SG11201610813TA (en) 2017-01-27
AU2015279719A1 (en) 2017-02-02
US9815828B2 (en) 2017-11-14
EP3160952B1 (en) 2020-12-02

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