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PE20211911A1 - Compuestos heterociclicos como inmunomoduladores - Google Patents

Compuestos heterociclicos como inmunomoduladores

Info

Publication number
PE20211911A1
PE20211911A1 PE2020001506A PE2020001506A PE20211911A1 PE 20211911 A1 PE20211911 A1 PE 20211911A1 PE 2020001506 A PE2020001506 A PE 2020001506A PE 2020001506 A PE2020001506 A PE 2020001506A PE 20211911 A1 PE20211911 A1 PE 20211911A1
Authority
PE
Peru
Prior art keywords
methyl
hydroxy
ethylamino
hydroxypyrrolidin
methylpyrrolidin
Prior art date
Application number
PE2020001506A
Other languages
English (en)
Inventor
Liangxing Wu
Jingwei Li
Wenqing Yao
Original Assignee
Incyte Corp
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 Incyte Corp filed Critical Incyte Corp
Publication of PE20211911A1 publication Critical patent/PE20211911A1/es

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    • 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
    • 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
    • A61K31/4353Heterocyclic 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
    • A61K31/437Heterocyclic 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
    • 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
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/28Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P33/00Antiparasitic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • A61P35/02Antineoplastic agents specific for leukemia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • A61P35/04Antineoplastic agents specific for metastasis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/02Immunomodulators
    • A61P37/04Immunostimulants
    • 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

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (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)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Immunology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Oncology (AREA)
  • Epidemiology (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Neurosurgery (AREA)
  • Communicable Diseases (AREA)
  • Psychiatry (AREA)
  • Hospice & Palliative Care (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Hematology (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)

Abstract

Esta referido a compuestos de Formula I', en donde: Anillo A es azetidinilo, pirrolidinilo o piperidinilo; X1 es CH o N; R1 es metilo o halo; R2 es alquilo, alcoxi, haloalquilo, haloalcoxi, entre otros; R3 es (R)-3-hidroxi-3-metilpirrolidin-1-ilo, (S)-3-hidroxi-3-metilpirrolidin-1-ilo, (R)-3-hidroxipirrolidin-1-ilo, (S)-3-hidroxipirrolidin-1-ilo, (R)-2-hidroxi-2-metil-etilamino, (S)-2-hidroxi-2-metil-etilamino, (R)-2-hidroxi-1-metil-etilamino y (S)-2-hidroxi-1-metil-etilamino; R4 es H, alquilo; R5 es COOH, CON(Ch3)2, entre otros. Entre los compuestos preferidos tenemos los siguientes: acido (R)-1-((7-ciano-2-(3'-(7-((3-hidroxipirrolidin-1-il)metil)-2-metilpirido[3,2-d]pirimidin-4-ilamino)-2,2'-dimetilbifenil-3-il)benzo[d]oxazol-5-il)metil)piperidin-4-carboxilico; acido (R)-1-((7-ciano-2-(3'-(7-((3-hidroxi-3-metilpirrolidin-1-il)metil)-2-metilpirido[3,2-d]pirimidin-4-ilamino)-2,2'-dimetilbifenil-3-il)benzo[d]oxazol-5-il)metil)piperidin-4-carboxilico; entre otros. Estos compuestos modulan la interaccion proteina/proteina PD-1/PD-L1 y son utiles en el tratamiento de diversas enfermedades que incluyen enfermedades infecciosas y cancer.
PE2020001506A 2018-03-30 2019-03-29 Compuestos heterociclicos como inmunomoduladores PE20211911A1 (es)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201862650821P 2018-03-30 2018-03-30
US201862687964P 2018-06-21 2018-06-21
PCT/US2019/025036 WO2019191707A1 (en) 2018-03-30 2019-03-29 Heterocyclic compounds as immunomodulators

Publications (1)

Publication Number Publication Date
PE20211911A1 true PE20211911A1 (es) 2021-09-28

Family

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PE2020001506A PE20211911A1 (es) 2018-03-30 2019-03-29 Compuestos heterociclicos como inmunomoduladores
PE2024002663A PE20251288A1 (es) 2018-03-30 2019-03-29 Compuestos heterociclicos como inmunomoduladores

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Country Status (34)

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US (4) US10669271B2 (es)
EP (3) EP4212529B1 (es)
JP (2) JP7372255B2 (es)
KR (2) KR102815634B1 (es)
CN (2) CN119613400A (es)
AU (2) AU2019245288C1 (es)
BR (1) BR112020019700A2 (es)
CA (1) CA3095758A1 (es)
CL (1) CL2020002511A1 (es)
CO (1) CO2020013601A2 (es)
CR (1) CR20200520A (es)
DK (2) DK4212529T3 (es)
EC (1) ECSP20069418A (es)
ES (2) ES3030010T3 (es)
FI (2) FI4212529T3 (es)
HR (2) HRP20250421T1 (es)
HU (1) HUE061258T2 (es)
IL (2) IL313101A (es)
LT (2) LT4212529T (es)
MA (1) MA64121B1 (es)
MD (1) MD3774791T2 (es)
MX (2) MX2020010321A (es)
PE (2) PE20211911A1 (es)
PH (1) PH12020551572A1 (es)
PL (2) PL3774791T3 (es)
PT (2) PT4212529T (es)
RS (2) RS66699B1 (es)
SG (1) SG11202009440WA (es)
SI (2) SI3774791T1 (es)
SM (2) SMT202300065T1 (es)
TW (1) TWI851563B (es)
UA (1) UA128453C2 (es)
WO (1) WO2019191707A1 (es)
ZA (1) ZA202403923B (es)

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