MX2021011118A - Derivados de azolopiridina macrocíclicos como moduladores de eed y prc2. - Google Patents

Derivados de azolopiridina macrocíclicos como moduladores de eed y prc2.

Info

Publication number
MX2021011118A
MX2021011118A MX2021011118A MX2021011118A MX2021011118A MX 2021011118 A MX2021011118 A MX 2021011118A MX 2021011118 A MX2021011118 A MX 2021011118A MX 2021011118 A MX2021011118 A MX 2021011118A MX 2021011118 A MX2021011118 A MX 2021011118A
Authority
MX
Mexico
Prior art keywords
sub
prc2
azolopyridine
eed
macrocyclic
Prior art date
Application number
MX2021011118A
Other languages
English (en)
Inventor
Ivan Viktorovich Efremov
Owen Brendan Wallace
Iii Lorin A Thompson
Peter Rahl
Steven Kazmirski
Qingyi Li
Shawn Donald Johnstone
Feng Zhou
Original Assignee
Fulcrum Therapeutics 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 Fulcrum Therapeutics Inc filed Critical Fulcrum Therapeutics Inc
Publication of MX2021011118A publication Critical patent/MX2021011118A/es

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/12—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains three hetero rings
    • C07D498/16—Peri-condensed systems
    • 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
    • A61K31/4353—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 ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/4355—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 ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having 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
    • 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
    • A61K31/4353—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 ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/437—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 ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
    • 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
    • A61K31/5365—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 ortho- or peri-condensed with heterocyclic ring systems
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • 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
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • 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
    • A61P7/06—Antianaemics
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
    • C07D491/12—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains three hetero rings
    • C07D491/18—Bridged systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
    • C07D491/22—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains four or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/22—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains four or more hetero rings

Abstract

La invención se refiere a moduladores del desarrollo de ectodermo embrionario (EED) y/o complejo represivo Polycomb 2 (PRC2) útiles en el tratamiento de trastornos y enfermedades asociados con EEC y PRC2, los cuales son derivados de azolopiridina macrocíclicos y composiciones de los mismos de la Fórmula I:(Ver Fòrmula I, o una sal, profármaco, solvato, hidrato, enantiómero, isómero o tautómero farmacéuticamente aceptable de los mismos, en donde X1, X2, X3, A1, A2, Y, R1, R2, R3 y R4 son como se describen en el presente documento.
MX2021011118A 2019-03-15 2020-03-13 Derivados de azolopiridina macrocíclicos como moduladores de eed y prc2. MX2021011118A (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US201962819064P 2019-03-15 2019-03-15
PCT/US2020/022724 WO2020190754A1 (en) 2019-03-15 2020-03-13 Macrocyclic azolopyridine derivatives as eed and prc2 modulators

Publications (1)

Publication Number Publication Date
MX2021011118A true MX2021011118A (es) 2022-01-18

Family

ID=70228838

Family Applications (1)

Application Number Title Priority Date Filing Date
MX2021011118A MX2021011118A (es) 2019-03-15 2020-03-13 Derivados de azolopiridina macrocíclicos como moduladores de eed y prc2.

Country Status (13)

Country Link
US (4) US10973805B2 (es)
EP (1) EP3938050A1 (es)
JP (1) JP2022525199A (es)
KR (1) KR20210151833A (es)
CN (1) CN114144230B (es)
AU (1) AU2020241254A1 (es)
BR (1) BR112021018238A2 (es)
CA (1) CA3133751A1 (es)
IL (1) IL286433A (es)
MX (1) MX2021011118A (es)
SG (1) SG11202110092PA (es)
TW (1) TW202102495A (es)
WO (1) WO2020190754A1 (es)

Families Citing this family (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CA3128468A1 (en) 2017-10-05 2019-04-11 Fulcrum Therapeutics, Inc. P38 kinase inhibitors reduce dux4 and downstream gene expression for the treatment of fshd
TW202102495A (zh) 2019-03-15 2021-01-16 美商弗爾康醫療公司 Ｅｅｄ及ｐｒｃ２調節劑之巨環唑并吡啶衍生物
EP4313993A1 (en) * 2021-04-02 2024-02-07 Fulcrum Therapeutics, Inc. Macrocyclic azolopyridines
WO2022212748A1 (en) * 2021-04-02 2022-10-06 Fulcrum Therapeutics, Inc. Polymorphic forms of (s)-12-fluoro-4-(1-methyl-1h-pyrazol-5-yl)-7a,8,13,14-tetrahydro-7h-[1,2,4]triazolo[4',3':1,6]pyrido[3,2-b]benzofuro[4,3-fg][1,4]oxazonine
CN115490708A (zh) * 2021-06-18 2022-12-20 苏州亚盛药业有限公司 磺酰胺类大环衍生物及其制备方法和用途
WO2023049724A1 (en) * 2021-09-24 2023-03-30 Oric Pharmaceuticals, Inc. Prc2 inhibitors for use in treating blood disorders
WO2023049723A1 (en) * 2021-09-24 2023-03-30 Oric Pharmaceuticals, Inc. Prc2 inhibitors for use in treating blood disorders
WO2023192415A1 (en) * 2022-03-29 2023-10-05 Fulcrum Therapeutics, Inc. An embryonic ectoderm development inhibitor for the treatment of sickle cell disease

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US5262564A (en) 1992-10-30 1993-11-16 Octamer, Inc. Sulfinic acid adducts of organo nitroso compounds useful as retroviral inactivating agents anti-retroviral agents and anti-tumor agents
CN103987842A (zh) * 2011-09-30 2014-08-13 葛兰素史密斯克莱有限责任公司 治疗癌症的方法
KR101987861B1 (ko) 2011-11-03 2019-06-11 밀레니엄 파머슈티컬스 인코퍼레이티드 Nedd-8 활성화 효소 억제제 및 저메틸화제의 투여
SG11201703880VA (en) * 2014-12-23 2017-07-28 Novartis Ag Triazolopyrimidine compounds and uses thereof
WO2017221092A1 (en) * 2016-06-20 2017-12-28 Novartis Ag Triazolopyridine compounds and uses thereof
CN109790166A (zh) * 2016-06-20 2019-05-21 诺华股份有限公司 咪唑并吡啶化合物用于治疗癌症
WO2018013929A1 (en) 2016-07-15 2018-01-18 Tufts Medical Center Compositions and methods for improving immune system function
EP3573618B1 (en) 2017-01-30 2023-08-16 The Children's Hospital of Philadelphia Compositions and methods for hemoglobin production
CN110740996B (zh) 2017-04-10 2024-01-09 密执安大学评议会 共价小分子dcn1抑制剂和使用其的治疗方法
UY37842A (es) * 2017-08-15 2019-03-29 Abbvie Inc Inhibidores de mcl-1 macrocíclicos y métodos de uso
US10342786B2 (en) 2017-10-05 2019-07-09 Fulcrum Therapeutics, Inc. P38 kinase inhibitors reduce DUX4 and downstream gene expression for the treatment of FSHD
MX2021005843A (es) 2018-11-20 2021-10-01 Fulcrum Therapeutics Inc Composiciones y métodos para aumentar la hemoglobina fetal y tratar la anemia de células falciformes.
TW202102495A (zh) 2019-03-15 2021-01-16 美商弗爾康醫療公司 Ｅｅｄ及ｐｒｃ２調節劑之巨環唑并吡啶衍生物
EP4313993A1 (en) 2021-04-02 2024-02-07 Fulcrum Therapeutics, Inc. Macrocyclic azolopyridines
WO2022212748A1 (en) 2021-04-02 2022-10-06 Fulcrum Therapeutics, Inc. Polymorphic forms of (s)-12-fluoro-4-(1-methyl-1h-pyrazol-5-yl)-7a,8,13,14-tetrahydro-7h-[1,2,4]triazolo[4',3':1,6]pyrido[3,2-b]benzofuro[4,3-fg][1,4]oxazonine
EP4329754A1 (en) 2021-04-29 2024-03-06 Fulcrum Therapeutics, Inc. Methods of regulating bcl11a expression and treatment of bcl11a-mediated disorders

Also Published As

Publication number Publication date
JP2022525199A (ja) 2022-05-11
US10973805B2 (en) 2021-04-13
BR112021018238A2 (pt) 2021-12-28
US20220160686A1 (en) 2022-05-26
US20240075016A1 (en) 2024-03-07
US11590111B2 (en) 2023-02-28
CN114144230A (zh) 2022-03-04
AU2020241254A1 (en) 2021-10-07
WO2020190754A1 (en) 2020-09-24
IL286433A (en) 2021-10-31
KR20210151833A (ko) 2021-12-14
US20240139163A1 (en) 2024-05-02
CN114144230B (zh) 2024-04-23
TW202102495A (zh) 2021-01-16
US20200360353A1 (en) 2020-11-19
CA3133751A1 (en) 2020-09-24
SG11202110092PA (en) 2021-10-28
EP3938050A1 (en) 2022-01-19

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