CA3149482A1 - Bis-[n-((5-carbamoyl)-1h-benzo[d]imidazol-2-yl)-pyrazol-5-carboxamide] derivatives and related compounds as sting (stimulator of interferon genes) agonists for the treatment of cancer - Google Patents

Bis-[n-((5-carbamoyl)-1h-benzo[d]imidazol-2-yl)-pyrazol-5-carboxamide] derivatives and related compounds as sting (stimulator of interferon genes) agonists for the treatment of cancer Download PDF

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Publication number
CA3149482A1
CA3149482A1 CA3149482A CA3149482A CA3149482A1 CA 3149482 A1 CA3149482 A1 CA 3149482A1 CA 3149482 A CA3149482 A CA 3149482A CA 3149482 A CA3149482 A CA 3149482A CA 3149482 A1 CA3149482 A1 CA 3149482A1
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Canada
Prior art keywords
alkyl
optionally substituted
alkoxy
amino
independently
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CA3149482A
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English (en)
French (fr)
Inventor
Jeremy R. Duvall
Keith W. Bentley
Brian D. Jones
Eugene W. Kelleher
Soumya S. RAY
Joshua D. Thomas
Dorin Toader
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Mersana Therapeutics Inc
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Mersana Therapeutics Inc
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Publication of CA3149482A1 publication Critical patent/CA3149482A1/en
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    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic 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
    • C07D471/02—Heterocyclic 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
    • C07D471/04—Ortho-condensed 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
    • A61K31/41—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
    • A61K31/4192—1,2,3-Triazoles
    • A—HUMAN NECESSITIES
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    • 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
    • A61K31/422—Oxazoles not condensed and containing further heterocyclic rings
    • A—HUMAN NECESSITIES
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    • 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
    • A61K31/425—Thiazoles
    • A61K31/427—Thiazoles not condensed and containing further heterocyclic rings
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    • 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
    • A61K31/4353—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 ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/4355—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 ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having oxygen as a ring hetero atom
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    • 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
    • A61K31/4353—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 ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/437—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 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
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    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing three or more hetero rings
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    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/14—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
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    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
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    • C07D417/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings
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    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
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    • C—CHEMISTRY; METALLURGY
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    • C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
    • C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
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    • C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
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    • 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

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  • Obesity (AREA)
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  • Pulmonology (AREA)
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  • Gastroenterology & Hepatology (AREA)
  • Child & Adolescent Psychology (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • AIDS & HIV (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • Transplantation (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
CA3149482A 2019-08-02 2020-07-31 Bis-[n-((5-carbamoyl)-1h-benzo[d]imidazol-2-yl)-pyrazol-5-carboxamide] derivatives and related compounds as sting (stimulator of interferon genes) agonists for the treatment of cancer Pending CA3149482A1 (en)

Applications Claiming Priority (7)

Application Number Priority Date Filing Date Title
US201962882081P 2019-08-02 2019-08-02
US62/882,081 2019-08-02
US201962944643P 2019-12-06 2019-12-06
US62/944,643 2019-12-06
US202062982935P 2020-02-28 2020-02-28
US62/982,935 2020-02-28
PCT/US2020/044538 WO2021026009A1 (en) 2019-08-02 2020-07-31 Bis-[n-((5-carbamoyl)-1h-benzo[d]imidazol-2-yl)-pyrazol-5-carboxamide] derivatives and related compounds as sting (stimulator of interferon genes) agonists for the treatment of cancer

Publications (1)

Publication Number Publication Date
CA3149482A1 true CA3149482A1 (en) 2021-02-11

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CA3149482A Pending CA3149482A1 (en) 2019-08-02 2020-07-31 Bis-[n-((5-carbamoyl)-1h-benzo[d]imidazol-2-yl)-pyrazol-5-carboxamide] derivatives and related compounds as sting (stimulator of interferon genes) agonists for the treatment of cancer

Country Status (13)

Country Link
US (3) US11155567B2 (enExample)
EP (1) EP4007758A1 (enExample)
JP (1) JP7843695B2 (enExample)
KR (1) KR20220056176A (enExample)
CN (1) CN114585623A (enExample)
AU (1) AU2020324388A1 (enExample)
BR (1) BR112022001931A2 (enExample)
CA (1) CA3149482A1 (enExample)
IL (1) IL290212A (enExample)
MX (2) MX2022001407A (enExample)
TW (1) TW202120500A (enExample)
WO (1) WO2021026009A1 (enExample)
ZA (1) ZA202201505B (enExample)

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IL296901A (en) * 2020-04-02 2022-12-01 Mersana Therapeutics Inc Antibody-drug conjugates comprising sting agonists
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WO2022177307A1 (ko) * 2021-02-17 2022-08-25 한국화학연구원 벤즈이미다졸 유도체를 유효 성분으로 포함하는 인터페론 유전자 자극제 조성물
WO2022247743A1 (en) * 2021-05-24 2022-12-01 Fulgent Genetics, Inc. Compounds and their use as vaccine adjuvants
TW202432101A (zh) * 2022-11-08 2024-08-16 韓商瑞嘉化學生物科學股份有限公司 Sting促效劑
WO2024174863A1 (zh) * 2023-02-22 2024-08-29 深圳众格生物科技有限公司 Sting激动剂及其制备方法和医药用途
JP2026508759A (ja) * 2023-02-27 2026-03-12 バイオンテック・エスイー ヒドラジド、ヒドラジン、及びヒドロキサム酸官能基を含有するｓｔｉｎｇアゴニスト
WO2024186626A1 (en) * 2023-03-03 2024-09-12 Bolt Biotherapeutics, Inc. Aza-bicyclic sting agonist immunoconjugates, and uses thereof
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CN117229310B (zh) * 2023-09-18 2026-03-31 上海皓元生物医药科技有限公司 一种sting激动剂及其中间体的制备方法
US20260053942A1 (en) 2024-05-30 2026-02-26 Astellas Pharama Inc. Sting agonist immunostimulatory antibody drug conjugates
WO2026078593A1 (en) 2024-10-08 2026-04-16 Sun Pharma Advanced Research Company Limited Sting agonists and antibody drug conjugates thereof

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