MX2020011564A - Analogos de rapamicina unidos a c26 como inhibidores de mtor. - Google Patents

Analogos de rapamicina unidos a c26 como inhibidores de mtor.

Info

Publication number
MX2020011564A
MX2020011564A MX2020011564A MX2020011564A MX2020011564A MX 2020011564 A MX2020011564 A MX 2020011564A MX 2020011564 A MX2020011564 A MX 2020011564A MX 2020011564 A MX2020011564 A MX 2020011564A MX 2020011564 A MX2020011564 A MX 2020011564A
Authority
MX
Mexico
Prior art keywords
binded
mtor inhibitors
rapamycin analogues
mtor
compounds
Prior art date
Application number
MX2020011564A
Other languages
English (en)
Spanish (es)
Inventor
Walter Won
Gert Kiss
Jennifer Pitzen
James Bradley Aggen
Arun P Thottumkara
Adrian Liam Gill
James Joseph Cregg
Gang Wang
Micah James Evans Gliedt
G Leslie Burnett
Christopher Michael Semko
Julie Chu- Li LEE
Original Assignee
Revolution Medicines 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 Revolution Medicines Inc filed Critical Revolution Medicines Inc
Publication of MX2020011564A publication Critical patent/MX2020011564A/es

Links

Classifications

    • 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
    • C07D498/18—Bridged 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
    • A61K31/47—Quinolines; Isoquinolines
    • A61K31/4738—Quinolines; Isoquinolines 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
    • 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
    • A61K31/495—Heterocyclic 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
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • 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
    • A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • A61K31/553—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having at least one nitrogen and one oxygen as ring hetero atoms, e.g. loxapine, staurosporine
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D519/00—Heterocyclic 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)
  • 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)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
MX2020011564A 2018-05-01 2019-04-29 Analogos de rapamicina unidos a c26 como inhibidores de mtor. MX2020011564A (es)

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
US201862665426P 2018-05-01 2018-05-01
US201862752881P 2018-10-30 2018-10-30
US201962836040P 2019-04-18 2019-04-18
PCT/US2019/029738 WO2019212991A1 (en) 2018-05-01 2019-04-29 C26-linked rapamycin analogs as mtor inhibitors

Publications (1)

Publication Number Publication Date
MX2020011564A true MX2020011564A (es) 2021-01-29

Family

ID=66625253

Family Applications (2)

Application Number Title Priority Date Filing Date
MX2020011564A MX2020011564A (es) 2018-05-01 2019-04-29 Analogos de rapamicina unidos a c26 como inhibidores de mtor.
MX2023007581A MX2023007581A (es) 2018-05-01 2020-10-30 Analogos de rapamicina unidos a c26 como inhibidores de mtor.

Family Applications After (1)

Application Number Title Priority Date Filing Date
MX2023007581A MX2023007581A (es) 2018-05-01 2020-10-30 Analogos de rapamicina unidos a c26 como inhibidores de mtor.

Country Status (11)

Country Link
US (2) US11685749B2 (OSRAM)
EP (1) EP3788050B1 (OSRAM)
JP (1) JP7381492B2 (OSRAM)
KR (1) KR102859103B1 (OSRAM)
CN (1) CN112368289B (OSRAM)
AU (2) AU2019262979B2 (OSRAM)
CA (1) CA3098698A1 (OSRAM)
IL (2) IL278335B2 (OSRAM)
MX (2) MX2020011564A (OSRAM)
SG (1) SG11202010560QA (OSRAM)
WO (1) WO2019212991A1 (OSRAM)

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