PE20230159A1 - Derivados de 3-(5-metoxi-1-oxoisoindolin-2-il)piperidin-2,6-diona y usos - Google Patents

Derivados de 3-(5-metoxi-1-oxoisoindolin-2-il)piperidin-2,6-diona y usos

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Publication number
PE20230159A1
PE20230159A1 PE2022001098A PE2022001098A PE20230159A1 PE 20230159 A1 PE20230159 A1 PE 20230159A1 PE 2022001098 A PE2022001098 A PE 2022001098A PE 2022001098 A PE2022001098 A PE 2022001098A PE 20230159 A1 PE20230159 A1 PE 20230159A1
Authority
PE
Peru
Prior art keywords
alkyl
oxoisoindolin
piperidin
methoxy
dione
Prior art date
Application number
PE2022001098A
Other languages
English (en)
Inventor
Simone Bonazzi
Artiom Cernijenko
Jennifer Stroka Cobb
Natalie Dales
John Ryan Kerrigan
Philip Lam
Hasnain Ahmed Malik
Gary O'brien
Andrew W Patterson
Noel Marie-France Thomsen
Pamela Ting
Original Assignee
Novartis Ag
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 Novartis Ag filed Critical Novartis Ag
Publication of PE20230159A1 publication Critical patent/PE20230159A1/es

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D413/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14Heterocyclic 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic 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
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445Non condensed piperidines, e.g. piperocaine
    • A61K31/4523Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/4545Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. pipamperone, anabasine
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic 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
    • A61K31/4965Non-condensed pyrazines
    • A61K31/497Non-condensed pyrazines containing further heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic 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
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/506Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/535Heterocyclic 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
    • A61K31/53751,4-Oxazines, e.g. morpholine
    • A61K31/53771,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00Drugs for disorders of the blood or the extracellular fluid
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00Drugs for disorders of the blood or the extracellular fluid
    • A61P7/06Antianaemics
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic 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
    • C07D401/02Heterocyclic 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
    • C07D401/12Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic 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
    • C07D401/14Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D405/00Heterocyclic 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
    • C07D405/14Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D417/00Heterocyclic 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
    • C07D417/14Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D471/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04Ortho-condensed systems

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Epidemiology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Hydrogenated Pyridines (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)

Abstract

La presente invencion se refiere a compuestos derivados de 3-(5-metoxi-1-oxoisoindolin-2-il)piperidin-2,6-diona de formula (I'); en donde Y es O, CH2, CF2, y CHF; z es de 0 a 2; RX1 y RX2 es cada uno, independientemente, H y alquilo C1-C6; RY1 y RY2 es cada uno, independientemente, H y alquilo C1-C6; RZ1 y RZ2 son ambos hidrogeno; R1 es H y alquilo C1-C6; R2 es H, -C(=O)-R3 , cicloalquilo C3-C8, haloalquilo C1-C6 y alquilo C1-C10. Un compuesto seleccionado es 3-(5-(((R)-1-((1-ciclohexil-1H-pirazol-4-il)metil) piperidin-2-il)metoxi)-1-oxoisoindolin-2- il)piperidin-2,6-diona. Tambien refiere a una composicion farmaceutica que los comprende. Dichos compuestos son efectivos para reducir los niveles de expresion de la proteina Motivos de Dedos de Zinc Ampliamente Interespaciados (WIZ) y/o para inducir la expresion de la hemoglobina fetal (HbF), siendo util en el tratamiento de trastornos sanguineos hereditarios (hemoglobinopatias, beta-hemoglobinopatias), tales como la enfermedad de celulas falciformes y la betatalasemia.
PE2022001098A 2019-12-18 2020-12-16 Derivados de 3-(5-metoxi-1-oxoisoindolin-2-il)piperidin-2,6-diona y usos PE20230159A1 (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US201962950048P 2019-12-18 2019-12-18
PCT/IB2020/062070 WO2021124172A1 (en) 2019-12-18 2020-12-16 3-(5-methoxy-1-oxoisoindolin-2-yl)piperidine-2,6-dione derivatives and uses thereof

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PE20230159A1 true PE20230159A1 (es) 2023-02-01

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US (1) US11566022B2 (es)
EP (1) EP4076650B1 (es)
JP (1) JP2023506642A (es)
KR (1) KR20220114065A (es)
CN (1) CN114828959B (es)
AR (1) AR120773A1 (es)
AU (1) AU2020410514A1 (es)
BR (1) BR112022011796A2 (es)
CA (1) CA3164832A1 (es)
CO (1) CO2022008243A2 (es)
CR (1) CR20220278A (es)
DO (1) DOP2022000121A (es)
EC (1) ECSP22055267A (es)
IL (1) IL293530A (es)
JO (1) JOP20220152A1 (es)
MX (1) MX2022007351A (es)
PE (1) PE20230159A1 (es)
TW (1) TW202130631A (es)
UY (1) UY38986A (es)
WO (1) WO2021124172A1 (es)

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* Cited by examiner, † Cited by third party
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UY39671A (es) 2021-03-15 2022-10-31 Novartis Ag Derivados de pirazolopiridina y sus usos.
PE20240657A1 (es) * 2021-06-03 2024-04-04 Novartis Ag Derivados de 3-(1-oxoisoindolin-2-il)piperidina-2,6-diona y sus usos medicos
WO2023006097A1 (zh) * 2021-07-30 2023-02-02 海创药业股份有限公司 一种双功能嵌合体杂环化合物及其作为雄激素受体降解剂的用途
CN115959976A (zh) * 2022-12-30 2023-04-14 安徽诺全药业有限公司 一种甲氧基取代双环戊烷衍生物的制备方法

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Publication number Publication date
CO2022008243A2 (es) 2022-07-08
US11566022B2 (en) 2023-01-31
AR120773A1 (es) 2022-03-16
IL293530A (en) 2022-08-01
CN114828959B (zh) 2024-04-02
CA3164832A1 (en) 2021-06-24
EP4076650B1 (en) 2024-02-28
EP4076650A1 (en) 2022-10-26
JOP20220152A1 (ar) 2023-01-30
AU2020410514A1 (en) 2022-06-30
US20220402904A1 (en) 2022-12-22
MX2022007351A (es) 2022-07-19
JP2023506642A (ja) 2023-02-17
UY38986A (es) 2021-07-30
ECSP22055267A (es) 2022-08-31
KR20220114065A (ko) 2022-08-17
DOP2022000121A (es) 2022-08-15
WO2021124172A1 (en) 2021-06-24
TW202130631A (zh) 2021-08-16
CN114828959A (zh) 2022-07-29
BR112022011796A2 (pt) 2022-08-30
CR20220278A (es) 2022-07-01

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