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JOP20190070A1 - مركبات بنزو[b] ثيوفين كناهضات محفزة لبروتين جينات الإنترفيرون - Google Patents

مركبات بنزو[b] ثيوفين كناهضات محفزة لبروتين جينات الإنترفيرون

Info

Publication number
JOP20190070A1
JOP20190070A1 JOP/2019/0070A JOP20190070A JOP20190070A1 JO P20190070 A1 JOP20190070 A1 JO P20190070A1 JO P20190070 A JOP20190070 A JO P20190070A JO P20190070 A1 JOP20190070 A1 JO P20190070A1
Authority
JO
Jordan
Prior art keywords
compounds
general formula
benzo
thiophene compounds
sting agonists
Prior art date
Application number
JOP/2019/0070A
Other languages
English (en)
Inventor
P Jewell James
Lim Jongwon
Lu Min
Liang Rui
D Altman Michael
Chang Wonsuk
Tyagarajan Sriram
Siu Tony
D Cash Brandon
N Cumming Jared
Wesley Trotter Benjamin
J Henderson Timothy
A Larsen Matthew
D Otte Ryan
M Haidle Andrew
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 JOP20190070A1 publication Critical patent/JOP20190070A1/ar
Application granted granted Critical
Publication of JOP20190070B1 publication Critical patent/JOP20190070B1/ar

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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)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (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)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Peptides Or Proteins (AREA)
  • Enzymes And Modification Thereof (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)

Abstract

يتعلق الاختراع الحالي بتوفير مركبات من الصيغة العامة (Ia)، مركبات من الصيغة العامة (Ia’)، مركبات من الصيغة العامة (Ib)، مركبات من الصيغة العامة (Ib’)، مركبات من الصيغة العامة (I)، مركبات من الصيغة العامة (I’)، وأملاح منها مقبولة صيدلانياً، حيث يتم هنا تحديد R1، R2، R3، R4، R5، R6، R8، R9، X1، X2، وX3، والتي قد تكون مفيدة بوصفها مُحثات لإنتاج إنترفيرون من النوع 1، بصفة خاصة كعوامل نشطة محفزة لبروتين جينات الإنترفيرون. يتم أيضاً توفير عمليات لتصنيع واستخدام مركبات الكشف.
JOP/2019/0070A 2016-10-04 2017-10-02 مركبات بنزو[b] ثيوفين كناهضات محفزة لبروتين جينات الإنترفيرون JOP20190070B1 (ar)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US201662404062P 2016-10-04 2016-10-04
PCT/US2017/054688 WO2018067423A1 (en) 2016-10-04 2017-10-02 BENZO[b]THIOPHENE COMPOUNDS AS STING AGONISTS

Publications (2)

Publication Number Publication Date
JOP20190070A1 true JOP20190070A1 (ar) 2019-04-04
JOP20190070B1 JOP20190070B1 (ar) 2023-09-17

Family

ID=60084122

Family Applications (1)

Application Number Title Priority Date Filing Date
JOP/2019/0070A JOP20190070B1 (ar) 2016-10-04 2017-10-02 مركبات بنزو[b] ثيوفين كناهضات محفزة لبروتين جينات الإنترفيرون

Country Status (39)

Country Link
US (3) US10414747B2 (ar)
EP (1) EP3523287B1 (ar)
JP (1) JP6636673B2 (ar)
KR (1) KR102312721B1 (ar)
CN (1) CN110036001B (ar)
AR (1) AR109788A1 (ar)
AU (1) AU2017339418C1 (ar)
CA (1) CA3038903C (ar)
CL (1) CL2019000902A1 (ar)
CO (1) CO2019003349A2 (ar)
CR (1) CR20190168A (ar)
CY (1) CY1124837T1 (ar)
DK (1) DK3523287T3 (ar)
DO (1) DOP2019000083A (ar)
EA (1) EA037626B1 (ar)
EC (1) ECSP19026680A (ar)
ES (1) ES2893532T3 (ar)
GE (1) GEP20217285B (ar)
HR (1) HRP20211617T1 (ar)
HU (1) HUE056502T2 (ar)
IL (1) IL265678B2 (ar)
JO (1) JOP20190070B1 (ar)
LT (1) LT3523287T (ar)
MA (1) MA46452B1 (ar)
MD (1) MD3523287T2 (ar)
MX (1) MX2019003829A (ar)
MY (1) MY196383A (ar)
NI (1) NI201900029A (ar)
PE (1) PE20190705A1 (ar)
PH (1) PH12019500712A1 (ar)
PL (1) PL3523287T3 (ar)
PT (1) PT3523287T (ar)
RS (1) RS62410B1 (ar)
SG (1) SG10202008647TA (ar)
SI (1) SI3523287T1 (ar)
TN (2) TN2020000158A1 (ar)
TW (1) TWI796306B (ar)
UA (1) UA125223C2 (ar)
WO (1) WO2018067423A1 (ar)

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