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PE20190705A1 - COMPUESTOS DE BENZO[b] TIOFENO COMO AGONISTAS DE STING - Google Patents

COMPUESTOS DE BENZO[b] TIOFENO COMO AGONISTAS DE STING

Info

Publication number
PE20190705A1
PE20190705A1 PE2019000764A PE2019000764A PE20190705A1 PE 20190705 A1 PE20190705 A1 PE 20190705A1 PE 2019000764 A PE2019000764 A PE 2019000764A PE 2019000764 A PE2019000764 A PE 2019000764A PE 20190705 A1 PE20190705 A1 PE 20190705A1
Authority
PE
Peru
Prior art keywords
thiophen
sting agonists
compounds
benzo compounds
haloalkyl
Prior art date
Application number
PE2019000764A
Other languages
English (en)
Inventor
Michael D Altman
Brandon D Cash
Wonsuk Chang
Jared N Cumming
Andrew M Haidle
Timothy J Henderson
James P Jewell
Matthew A Larsen
Rui Liang
Jongwon Lim
Min Lu
Ryan D Otte
Tony Siu
Benjamin Wesley Trotter
Sriram Tyagarajan
Original Assignee
Merck Sharp & Dohme
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 Merck Sharp & Dohme filed Critical Merck Sharp & Dohme
Publication of PE20190705A1 publication Critical patent/PE20190705A1/es

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D333/00—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom
    • C07D333/50—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom condensed with carbocyclic rings or ring systems
    • C07D333/52—Benzo[b]thiophenes; Hydrogenated benzo[b]thiophenes
    • C07D333/54—Benzo[b]thiophenes; Hydrogenated benzo[b]thiophenes with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to carbon atoms of the hetero ring
    • C07D333/60—Radicals substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • 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
    • A61K31/38—Heterocyclic compounds having sulfur as a ring hetero atom
    • A61K31/381—Heterocyclic compounds having sulfur as a ring hetero atom having five-membered 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
    • A61K31/38—Heterocyclic compounds having sulfur as a ring hetero atom
    • A61K31/385—Heterocyclic compounds having sulfur as a ring hetero atom having two or more sulfur atoms in the same ring
    • 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
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/42—Oxazoles
    • A61K31/424—Oxazoles condensed with heterocyclic ring systems, e.g. clavulanic acid
    • 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
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A61P37/04—Immunostimulants
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D333/00—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom
    • C07D333/50—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom condensed with carbocyclic rings or ring systems
    • C07D333/52—Benzo[b]thiophenes; Hydrogenated benzo[b]thiophenes
    • C07D333/62—Benzo[b]thiophenes; Hydrogenated benzo[b]thiophenes with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to carbon atoms of the hetero ring
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
    • C07D409/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
    • 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
    • C07D498/02—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 two hetero rings
    • C07D498/04—Ortho-condensed systems

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Immunology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Epidemiology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Enzymes And Modification Thereof (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Peptides Or Proteins (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)

Abstract

Se refiere a un compuesto de formula (Ia') o su sal farmaceuticamente aceptable, donde: R1 es H, halogeno, entre otros; R2 es H, CN, entre otros; R3 es H, COOR6, entre otros; R4 es H, OR6, entre otros; R5 es H, N(R6)2, entre otros; R6 es H, alquilo C1-C6, y haloalquilo C1-C6, pudiendo estar los 2 ultimos sustituidos con OH, O(alquilo C1-C3), y O(haloalquilo C1-C3); X1 es C(O); X2 es (C(R8)2)(1-3); R8 es H, CN, entre otros; y X3 es C(S)OR6, SO2R6, entre otros. Tambien se refiere a composiciones farmaceuticas que comprenden al compuesto de la invencion y a metodos de preparacion. Dichos compuestos son agonistas de STING (estimulador de genes de interferon) y son utiles en el tratamiento de enfermedades como el cancer
PE2019000764A 2016-10-04 2017-10-02 COMPUESTOS DE BENZO[b] TIOFENO COMO AGONISTAS DE STING PE20190705A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US201662404062P 2016-10-04 2016-10-04

Publications (1)

Publication Number Publication Date
PE20190705A1 true PE20190705A1 (es) 2019-05-17

Family

ID=60084122

Family Applications (1)

Application Number Title Priority Date Filing Date
PE2019000764A PE20190705A1 (es) 2016-10-04 2017-10-02 COMPUESTOS DE BENZO[b] TIOFENO COMO AGONISTAS DE STING

Country Status (39)

Country Link
US (3) US10414747B2 (es)
EP (1) EP3523287B1 (es)
JP (1) JP6636673B2 (es)
KR (1) KR102312721B1 (es)
CN (1) CN110036001B (es)
AR (1) AR109788A1 (es)
AU (1) AU2017339418C1 (es)
CA (1) CA3038903C (es)
CL (1) CL2019000902A1 (es)
CO (1) CO2019003349A2 (es)
CR (1) CR20190168A (es)
CY (1) CY1124837T1 (es)
DK (1) DK3523287T3 (es)
DO (1) DOP2019000083A (es)
EA (1) EA037626B1 (es)
EC (1) ECSP19026680A (es)
ES (1) ES2893532T3 (es)
GE (2) GEP20217285B (es)
HR (1) HRP20211617T1 (es)
HU (1) HUE056502T2 (es)
IL (1) IL265678B2 (es)
JO (1) JOP20190070B1 (es)
LT (1) LT3523287T (es)
MA (1) MA46452B1 (es)
MD (1) MD3523287T2 (es)
MX (1) MX386187B (es)
MY (1) MY196383A (es)
NI (1) NI201900029A (es)
PE (1) PE20190705A1 (es)
PH (1) PH12019500712B1 (es)
PL (1) PL3523287T3 (es)
PT (1) PT3523287T (es)
RS (1) RS62410B1 (es)
SG (1) SG10202008647TA (es)
SI (1) SI3523287T1 (es)
TN (2) TN2020000159A1 (es)
TW (1) TWI796306B (es)
UA (1) UA125223C2 (es)
WO (1) WO2018067423A1 (es)

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