BR112021018238A2 - Derivados de azolopiridina macrocíclicos como moduladores de eed e prc2 - Google Patents

Derivados de azolopiridina macrocíclicos como moduladores de eed e prc2

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Publication number
BR112021018238A2
BR112021018238A2 BR112021018238A BR112021018238A BR112021018238A2 BR 112021018238 A2 BR112021018238 A2 BR 112021018238A2 BR 112021018238 A BR112021018238 A BR 112021018238A BR 112021018238 A BR112021018238 A BR 112021018238A BR 112021018238 A2 BR112021018238 A2 BR 112021018238A2
Authority
BR
Brazil
Prior art keywords
prc2
azolopyridine
eed
modulators
macrocyclic
Prior art date
Application number
BR112021018238A
Other languages
English (en)
Inventor
Feng Zhou
Viktorovich Efremov Ivan
A Thompson Lorin Iii
Brendan Wallace Owen
Peter Rahl
Qingyi Li
Donald JOHNSTONE Shawn
Steven Kazmirski
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 BR112021018238A2 publication Critical patent/BR112021018238A2/pt

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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

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  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Epidemiology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Hematology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Diabetes (AREA)
  • Engineering & Computer Science (AREA)
  • Oncology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Enzymes And Modification Thereof (AREA)
  • Medicinal Preparation (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Telescopes (AREA)

Abstract

derivados de azolopiridina macrocíclicos como moduladores de eed e prc2. a presente invenção refere-se a moduladores do desenvolvimento do ectoderma embrionário (eed) e/ou complexo repressivo polycomb 2 (prc2) úteis no tratamento de distúrbios e doenças associados com eec e prc2, sendo derivados macrocíclicos de azolopiridina e composições dos mesmos de fórmula (i), ou um sal farmaceuticamente aceitável, pró-fármaco, solvato, hidrato, enantiômero, isômero ou tautômero do mesmo, em que x1, x2, x3, a1, a2, y, r1, r2, r3 e r4 são como aqui descritos.
BR112021018238A 2019-03-15 2020-03-13 Derivados de azolopiridina macrocíclicos como moduladores de eed e prc2 BR112021018238A2 (pt)

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
BR112021018238A2 true BR112021018238A2 (pt) 2021-12-28

Family

ID=70228838

Family Applications (1)

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BR112021018238A BR112021018238A2 (pt) 2019-03-15 2020-03-13 Derivados de azolopiridina macrocíclicos como moduladores de eed e prc2

Country Status (13)

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

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AU2018346712B2 (en) 2017-10-05 2021-04-01 Fulcrum Therapeutics, Inc. P38 kinase inhibitors reduce DUX4 and downstream gene expression for the treatment of FSHD
SG11202110092PA (en) 2019-03-15 2021-10-28 Fulcrum Therapeutics Inc Macrocyclic azolopyridine derivatives as eed and prc2 modulators
EP4313992A1 (en) * 2021-04-02 2024-02-07 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
KR20240056457A (ko) * 2021-04-02 2024-04-30 풀크럼 쎄러퓨틱스, 인코포레이티드 마크로사이클릭 아졸로피리딘
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
WO2023049723A1 (en) * 2021-09-24 2023-03-30 Oric Pharmaceuticals, Inc. Prc2 inhibitors for use in treating blood disorders
WO2023049724A1 (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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RU2014117632A (ru) * 2011-09-30 2015-11-10 ГЛЭКСОСМИТКЛАЙН ЭлЭлСи Способы лечения злокачественной опухоли
GEP20196940B (en) 2011-11-03 2019-01-10 Millennium Pharm Inc Administration d’un inhibiteur d’enzyme activant nedd8 et agent d’hypométhylation
ES2722048T3 (es) * 2014-12-23 2019-08-07 Novartis Ag Compuestos de triazolopirimidina y usos de los mismos
EP3472166A1 (en) * 2016-06-20 2019-04-24 Novartis AG Imidazopyrimidine compounds useful for the treatment of cancer
CN109906224B (zh) * 2016-06-20 2022-02-25 诺华股份有限公司 三唑吡啶化合物及其应用
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US11179379B2 (en) 2017-01-30 2021-11-23 The Children's Hospital Of Philadelphia Compositions and methods for hemoglobin production
JP7086171B2 (ja) 2017-04-10 2022-06-17 ザ リージェンツ オブ ザ ユニヴァシティ オブ ミシガン 共有結合性小分子ｄｃｎ１阻害物質およびそれを使用する治療方法
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SG11202110092PA (en) 2019-03-15 2021-10-28 Fulcrum Therapeutics Inc Macrocyclic azolopyridine derivatives as eed and prc2 modulators
EP4313992A1 (en) 2021-04-02 2024-02-07 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
KR20240056457A (ko) 2021-04-02 2024-04-30 풀크럼 쎄러퓨틱스, 인코포레이티드 마크로사이클릭 아졸로피리딘
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Also Published As

Publication number Publication date
US20220160686A1 (en) 2022-05-26
US20200360353A1 (en) 2020-11-19
CN114144230B (zh) 2024-04-23
TW202102495A (zh) 2021-01-16
AU2020241254A1 (en) 2021-10-07
US20240075016A1 (en) 2024-03-07
CA3133751A1 (en) 2020-09-24
EP3938050A1 (en) 2022-01-19
CN114144230A (zh) 2022-03-04
SG11202110092PA (en) 2021-10-28
US10973805B2 (en) 2021-04-13
KR20210151833A (ko) 2021-12-14
WO2020190754A1 (en) 2020-09-24
IL286433A (en) 2021-10-31
MX2021011118A (es) 2022-01-18
US11590111B2 (en) 2023-02-28
JP2022525199A (ja) 2022-05-11
US20240139163A1 (en) 2024-05-02

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