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PE20211444A1 - Componentes heterociclicos biciclicos sustituidos como inhibidores de prmt5 - Google Patents

Componentes heterociclicos biciclicos sustituidos como inhibidores de prmt5

Info

Publication number
PE20211444A1
PE20211444A1 PE2020000761A PE2020000761A PE20211444A1 PE 20211444 A1 PE20211444 A1 PE 20211444A1 PE 2020000761 A PE2020000761 A PE 2020000761A PE 2020000761 A PE2020000761 A PE 2020000761A PE 20211444 A1 PE20211444 A1 PE 20211444A1
Authority
PE
Peru
Prior art keywords
substituted
unsubstituted alkyl
halogen
independently selected
bicycle
Prior art date
Application number
PE2020000761A
Other languages
English (en)
Inventor
Prathap Sreedharan Nair
Ganesh Bhausaheb Gudade
Sachin Sethi
Dipak Raychand Lagad
Chetan Sanjay Pawar
Mahadeo Bhaskar Tryambake
Chaitanya Prabhakar Kulkarni
Anil Kashiram Hajare
Balasaheb Arjun Gore
Sanjeev Anant Kulkarni
Milind Dattatraya Sindkhedkar
Venkata P Palle
Rajender Kumar Kamboj
Original Assignee
Lupin Ltd
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 Lupin Ltd filed Critical Lupin Ltd
Publication of PE20211444A1 publication Critical patent/PE20211444A1/es

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Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D487/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04Ortho-condensed systems
    • 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
    • A61K31/47Quinolines; Isoquinolines
    • A61K31/4709Non-condensed quinolines 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
    • A61K31/495Heterocyclic 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
    • A61K31/519Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D519/00Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Epidemiology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)

Abstract

Referido a un compuesto que tiene la formula general I, un estereoisomero del mismo o una sal farmaceuticamente aceptable del mismo; en donde, L1 se selecciona entre -CRaRb-, -NRa-, S y O; Z se selecciona entre CH y N; Ra y Rb se seleccionan independientemente en cada aparicion entre H, alquilo sustituido o sin sustituir, entre otros; R se selecciona entre -NR4R5, H, halogeno, entre otros; R1 y R2, junto con los atomos de carbono a los que estan unidos, forman un enlace para formar un -C=C-; R2 y R2a, que pueden ser iguales o diferentes y se seleccionan independientemente entre H y alquilo sustituido o sin sustituir; R3 se selecciona independientemente en cada aparicion entre halogeno, ciano, nitro, alquilo sustituido o sin sustituir, R10 se selecciona entre hidrogeno, halogeno y alquilo sustituido o sin sustituir, entre otros; "n" es un numero entero que varia de 0 a 4. Un compuesto seleccionado es (1S,2R,5R)-3-(2-(2-Amino-3-bromoquinolin-7-il)etil)-5-(4-amino-7H-pirrolo[2,3-d]pirimidin-7-il)ciclopent-3-eno-1,2-diol. Estos componentes biciclicos sustituidos son inhibidores de PRMT5. Tambien se refiere a productos intermedios, metodos de su sintesis, y a composiciones farmaceuticas y su uso en el tratamiento de enfermedades, trastornos o afecciones asociados con la sobreexpresion de la enzima PRMT5, tales como glioblastoma multiforme, cancer de prostata, cancer de pancreas.
PE2020000761A 2017-12-13 2018-12-13 Componentes heterociclicos biciclicos sustituidos como inhibidores de prmt5 PE20211444A1 (es)

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
IN201721044886 2017-12-13
IN201821024634 2018-07-02
IN201821040029 2018-10-23
PCT/IB2018/060015 WO2019116302A1 (en) 2017-12-13 2018-12-13 Substituted bicyclic heterocyclic compounds as prmt5 inhibitors

Publications (1)

Publication Number Publication Date
PE20211444A1 true PE20211444A1 (es) 2021-08-05

Family

ID=65036860

Family Applications (1)

Application Number Title Priority Date Filing Date
PE2020000761A PE20211444A1 (es) 2017-12-13 2018-12-13 Componentes heterociclicos biciclicos sustituidos como inhibidores de prmt5

Country Status (30)

Country Link
US (2) US11459330B2 (es)
EP (1) EP3724190B1 (es)
JP (1) JP7282778B2 (es)
KR (1) KR102708147B1 (es)
CN (1) CN111712498B (es)
AU (1) AU2018385664B2 (es)
BR (1) BR112020011746A2 (es)
CA (1) CA3085259A1 (es)
CL (1) CL2020001576A1 (es)
CR (1) CR20200263A (es)
CU (1) CU24621B1 (es)
DK (1) DK3724190T3 (es)
ES (1) ES2927860T3 (es)
GE (1) GEP20227359B (es)
HR (1) HRP20221207T1 (es)
HU (1) HUE059945T2 (es)
IL (1) IL274936B2 (es)
LT (1) LT3724190T (es)
MX (1) MX2020006181A (es)
NZ (1) NZ765656A (es)
PE (1) PE20211444A1 (es)
PH (1) PH12020550881A1 (es)
PL (1) PL3724190T3 (es)
PT (1) PT3724190T (es)
RS (1) RS63623B1 (es)
SG (1) SG11202004934QA (es)
SM (1) SMT202200396T1 (es)
UA (1) UA126349C2 (es)
WO (1) WO2019116302A1 (es)
ZA (1) ZA202003528B (es)

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Publication number Publication date
JP7282778B2 (ja) 2023-05-29
ZA202003528B (en) 2022-05-25
MX2020006181A (es) 2020-09-03
KR102708147B1 (ko) 2024-09-19
CN111712498A (zh) 2020-09-25
GEP20227359B (en) 2022-03-10
US11459330B2 (en) 2022-10-04
HRP20221207T1 (hr) 2022-12-09
AU2018385664B2 (en) 2022-06-02
US20220267339A1 (en) 2022-08-25
CN111712498B (zh) 2023-09-29
EP3724190B1 (en) 2022-07-06
CA3085259A1 (en) 2019-06-20
CR20200263A (es) 2020-07-26
SMT202200396T1 (it) 2022-11-18
IL274936A (en) 2020-07-30
PL3724190T3 (pl) 2022-10-31
CL2020001576A1 (es) 2020-11-06
BR112020011746A2 (pt) 2020-11-17
UA126349C2 (uk) 2022-09-21
RS63623B1 (sr) 2022-10-31
DK3724190T3 (da) 2022-10-10
AU2018385664A1 (en) 2020-07-02
CU20200051A7 (es) 2021-03-11
KR20200098598A (ko) 2020-08-20
US11952380B2 (en) 2024-04-09
EP3724190A1 (en) 2020-10-21
NZ765656A (en) 2025-02-28
WO2019116302A1 (en) 2019-06-20
ES2927860T3 (es) 2022-11-11
US20210163486A1 (en) 2021-06-03
IL274936B1 (en) 2023-05-01
SG11202004934QA (en) 2020-07-29
PT3724190T (pt) 2022-10-03
JP2021506793A (ja) 2021-02-22
LT3724190T (lt) 2022-10-10
HUE059945T2 (hu) 2023-01-28
IL274936B2 (en) 2023-09-01
PH12020550881A1 (en) 2021-04-05
CU24621B1 (es) 2022-09-08

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