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BR112019006816A2 - compostos de benzo[b]tiofeno como agonistas de sting, composição farmacêutica e uso dos mesmos - Google Patents

compostos de benzo[b]tiofeno como agonistas de sting, composição farmacêutica e uso dos mesmos

Info

Publication number
BR112019006816A2
BR112019006816A2 BR112019006816A BR112019006816A BR112019006816A2 BR 112019006816 A2 BR112019006816 A2 BR 112019006816A2 BR 112019006816 A BR112019006816 A BR 112019006816A BR 112019006816 A BR112019006816 A BR 112019006816A BR 112019006816 A2 BR112019006816 A2 BR 112019006816A2
Authority
BR
Brazil
Prior art keywords
compounds
formula
benzo
pharmaceutical compositions
thiophene compounds
Prior art date
Application number
BR112019006816A
Other languages
English (en)
Other versions
BR112019006816B1 (pt
BR112019006816A8 (pt
Inventor
M Haidle Andrew
Wesley Trotter Benjamin
D Cash Brandon
P Jewell James
N Cumming Jared
Lim Jongwon
A Larsen Matthew
D Altman Michael
Lu Min
Liang Rui
D Otte Ryan
Tyagarajan Sriram
J Henderson Timothy
Siu Tony
Chang Wonsuk
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 BR112019006816A2 publication Critical patent/BR112019006816A2/pt
Publication of BR112019006816A8 publication Critical patent/BR112019006816A8/pt
Publication of BR112019006816B1 publication Critical patent/BR112019006816B1/pt

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D333/00Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom
    • C07D333/50Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom condensed with carbocyclic rings or ring systems
    • C07D333/52Benzo[b]thiophenes; Hydrogenated benzo[b]thiophenes
    • C07D333/54Benzo[b]thiophenes; Hydrogenated benzo[b]thiophenes with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to carbon atoms of the hetero ring
    • C07D333/60Radicals substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/38Heterocyclic compounds having sulfur as a ring hetero atom
    • A61K31/381Heterocyclic compounds having sulfur as a ring hetero atom having five-membered 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
    • A61K31/38Heterocyclic compounds having sulfur as a ring hetero atom
    • A61K31/385Heterocyclic compounds having sulfur as a ring hetero atom having two or more sulfur atoms in the same ring
    • 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
    • A61K31/41Heterocyclic 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
    • A61K31/42Oxazoles
    • A61K31/424Oxazoles condensed with heterocyclic ring systems, e.g. clavulanic acid
    • 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
    • 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
    • C07D333/00Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom
    • C07D333/50Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom condensed with carbocyclic rings or ring systems
    • C07D333/52Benzo[b]thiophenes; Hydrogenated benzo[b]thiophenes
    • C07D333/62Benzo[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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D409/00Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/02Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
    • C07D409/12Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D498/00Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/02Heterocyclic 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
    • C07D498/04Ortho-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

compostos de fórmula geral (ia), compostos de fórmula geral (ia?), compostos de fórmula geral (ib), compostos de fórmula geral (ib?), compostos de fórmula geral (i), compostos de fórmula geral (i?) e seus sais farmaceuticamente aceitáveis, em que r1, r2, r3, r4, r5, r6, r8, r9, x1, x2 e x3 são definidos aqui, que podem ser úteis como indutores da produção de interferon do tipo i, especificamente como agentes ativos de sting, são fornecidos. também são fornecidos processos para a síntese e uso dos compostos da invenção.
BR112019006816-3A 2016-10-04 2017-10-02 COMPOSTOS DE BENZO[b]TIOFENO COMO AGONISTAS DE STING BR112019006816B1 (pt)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201662404062P 2016-10-04 2016-10-04
US62/404,062 2016-10-04
PCT/US2017/054688 WO2018067423A1 (en) 2016-10-04 2017-10-02 BENZO[b]THIOPHENE COMPOUNDS AS STING AGONISTS

Publications (3)

Publication Number Publication Date
BR112019006816A2 true BR112019006816A2 (pt) 2019-07-30
BR112019006816A8 BR112019006816A8 (pt) 2023-02-07
BR112019006816B1 BR112019006816B1 (pt) 2024-09-24

Family

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Also Published As

Publication number Publication date
CO2019003349A2 (es) 2019-04-12
IL265678B2 (en) 2023-06-01
SG10202008647TA (en) 2020-10-29
UA125223C2 (uk) 2022-02-02
CY1124837T1 (el) 2022-11-25
CA3038903C (en) 2021-07-27
MA46452A (fr) 2021-04-07
LT3523287T (lt) 2021-11-10
NI201900029A (es) 2019-05-13
ECSP19026680A (es) 2019-04-30
US20180093964A1 (en) 2018-04-05
EP3523287B1 (en) 2021-09-01
MX2019003829A (es) 2019-07-01
US10730849B2 (en) 2020-08-04
JOP20190070B1 (ar) 2023-09-17
PL3523287T3 (pl) 2021-12-20
PT3523287T (pt) 2021-10-06
CN110036001B (zh) 2022-03-22
EP3523287A1 (en) 2019-08-14
ES2893532T3 (es) 2022-02-09
US10703738B2 (en) 2020-07-07
KR20190056432A (ko) 2019-05-24
US20190337917A1 (en) 2019-11-07
CR20190168A (es) 2019-05-17
TN2020000159A1 (en) 2022-04-04
CN110036001A (zh) 2019-07-19
EA037626B1 (ru) 2021-04-22
JOP20190070A1 (ar) 2019-04-04
MY196383A (en) 2023-03-28
WO2018067423A1 (en) 2018-04-12
DOP2019000083A (es) 2019-07-15
TN2020000158A1 (en) 2022-04-04
HUE056502T2 (hu) 2022-02-28
HRP20211617T1 (hr) 2022-03-04
GEAP202115066A (en) 2021-04-12
CL2019000902A1 (es) 2019-06-21
JP2019534876A (ja) 2019-12-05
SI3523287T1 (sl) 2021-11-30
CA3038903A1 (en) 2018-04-12
AU2017339418A1 (en) 2019-04-18
US10414747B2 (en) 2019-09-17
TWI796306B (zh) 2023-03-21
MD3523287T2 (ro) 2021-12-31
AU2017339418C1 (en) 2020-12-17
IL265678A (en) 2019-05-30
PE20190705A1 (es) 2019-05-17
AR109788A1 (es) 2019-01-23
AU2017339418B2 (en) 2020-04-16
BR112019006816A8 (pt) 2023-02-07
US20190337918A1 (en) 2019-11-07
TW201817723A (zh) 2018-05-16
RS62410B1 (sr) 2021-10-29
GEP20217285B (en) 2021-08-10
PH12019500712B1 (en) 2023-05-10
MA46452B1 (fr) 2021-10-29
DK3523287T3 (da) 2021-10-18
MX386187B (es) 2025-03-18
EA201990846A1 (ru) 2019-08-30
PH12019500712A1 (en) 2019-12-02
KR102312721B1 (ko) 2021-10-13
JP6636673B2 (ja) 2020-01-29

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Legal Events

Date Code Title Description
B07D Technical examination (opinion) related to article 229 of industrial property law [chapter 7.4 patent gazette]

Free format text: DE ACORDO COM O ARTIGO 229-C DA LEI N? 10196/2001, QUE MODIFICOU A LEI N? 9279/96, A CONCESS?O DA PATENTE EST? CONDICIONADA ? ANU?NCIA PR?VIA DA ANVISA. CONSIDERANDO A APROVA??O DOS TERMOS DO PARECER N? 337/PGF/EA/2010, BEM COMO A PORTARIA INTERMINISTERIAL N? 1065 DE 24/05/2012, ENCAMINHA-SE O PRESENTE PEDIDO PARA AS PROVID?NCIAS CAB?VEIS.

B07E Notification of approval relating to section 229 industrial property law [chapter 7.5 patent gazette]
B06W Patent application suspended after preliminary examination (for patents with searches from other patent authorities) chapter 6.23 patent gazette]
B350 Update of information on the portal [chapter 15.35 patent gazette]
B25A Requested transfer of rights approved

Owner name: MERCK SHARP AND DOHME LLC (US)

B09A Decision: intention to grant [chapter 9.1 patent gazette]
B16A Patent or certificate of addition of invention granted [chapter 16.1 patent gazette]

Free format text: PRAZO DE VALIDADE: 20 (VINTE) ANOS CONTADOS A PARTIR DE 02/10/2017, OBSERVADAS AS CONDICOES LEGAIS