CN111918871A - 基于环戊烷的sting(干扰素基因刺激物)调节剂 - Google Patents

基于环戊烷的sting(干扰素基因刺激物)调节剂 Download PDF

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Publication number
CN111918871A
CN111918871A CN201980019494.9A CN201980019494A CN111918871A CN 111918871 A CN111918871 A CN 111918871A CN 201980019494 A CN201980019494 A CN 201980019494A CN 111918871 A CN111918871 A CN 111918871A
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China
Prior art keywords
cancer
compound
salt
nmr
dmso
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Pending
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CN201980019494.9A
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English (en)
Chinese (zh)
Inventor
M·J·威思
I·J·麦卡尔平
R·帕特曼
E·Y·芮
A·芬萨姆
A·马代尔纳
M·贾莱
K·S·加吉瓦拉
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Pfizer Inc
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Pfizer Inc
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Publication of CN111918871A publication Critical patent/CN111918871A/zh
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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07FACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F9/00Compounds containing elements of Groups 5 or 15 of the Periodic Table
    • C07F9/02Phosphorus compounds
    • C07F9/547Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
    • C07F9/6564Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having phosphorus atoms, with or without nitrogen, oxygen, sulfur, selenium or tellurium atoms, as ring hetero atoms
    • C07F9/6571Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having phosphorus atoms, with or without nitrogen, oxygen, sulfur, selenium or tellurium atoms, as ring hetero atoms having phosphorus and oxygen atoms as the only ring hetero atoms
    • C07F9/6574Esters of oxyacids of phosphorus
    • C07F9/65744Esters of oxyacids of phosphorus condensed with carbocyclic or heterocyclic rings or ring systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07HSUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
    • C07H19/00Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro-derivatives thereof
    • C07H19/02Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro-derivatives thereof sharing nitrogen
    • C07H19/04Heterocyclic radicals containing only nitrogen atoms as ring hetero atom
    • C07H19/23Heterocyclic radicals containing two or more heterocyclic rings condensed among themselves or condensed with a common carbocyclic ring system, not provided for in groups C07H19/14 - C07H19/22
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/70Carbohydrates; Sugars; Derivatives thereof
    • A61K31/7042Compounds having saccharide radicals and heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/50Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
    • A61K47/51Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent
    • A61K47/68Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an antibody, an immunoglobulin or a fragment thereof, e.g. an Fc-fragment
    • A61K47/6801Drug-antibody or immunoglobulin conjugates defined by the pharmacologically or therapeutically active agent
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07HSUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
    • C07H19/00Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro-derivatives thereof
    • C07H19/02Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro-derivatives thereof sharing nitrogen
    • C07H19/04Heterocyclic radicals containing only nitrogen atoms as ring hetero atom
    • C07H19/16Purine radicals
    • C07H19/20Purine radicals with the saccharide radical esterified by phosphoric or polyphosphoric acids
    • C07H19/213Purine radicals with the saccharide radical esterified by phosphoric or polyphosphoric acids containing cyclic phosphate

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  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Molecular Biology (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Animal Behavior & Ethology (AREA)
  • Biochemistry (AREA)
  • Genetics & Genomics (AREA)
  • Biotechnology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Epidemiology (AREA)
  • Immunology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Medicinal Preparation (AREA)
  • Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)
  • Saccharide Compounds (AREA)
CN201980019494.9A 2018-03-15 2019-03-12 基于环戊烷的sting(干扰素基因刺激物)调节剂 Pending CN111918871A (zh)

Applications Claiming Priority (9)

Application Number Priority Date Filing Date Title
US201862643467P 2018-03-15 2018-03-15
US62/643,467 2018-03-15
US201862666204P 2018-05-03 2018-05-03
US62/666,204 2018-05-03
US201862742532P 2018-10-08 2018-10-08
US62/742,532 2018-10-08
US201962809990P 2019-02-25 2019-02-25
US62/809,990 2019-02-25
PCT/IB2019/052009 WO2019175776A1 (en) 2018-03-15 2019-03-12 Cyclopentane-based modulators of sting (stimulator of interferon genes)

Publications (1)

Publication Number Publication Date
CN111918871A true CN111918871A (zh) 2020-11-10

Family

ID=66103038

Family Applications (1)

Application Number Title Priority Date Filing Date
CN201980019494.9A Pending CN111918871A (zh) 2018-03-15 2019-03-12 基于环戊烷的sting(干扰素基因刺激物)调节剂

Country Status (25)

Country Link
US (4) US10538542B2 (https=)
EP (1) EP3765474B1 (https=)
JP (1) JP7266942B2 (https=)
KR (1) KR20200131878A (https=)
CN (1) CN111918871A (https=)
AU (1) AU2019234043A1 (https=)
BR (1) BR112020018593A2 (https=)
CA (1) CA3093631C (https=)
CL (1) CL2020002352A1 (https=)
CR (1) CR20200382A (https=)
DO (1) DOP2020000160A (https=)
EC (1) ECSP20057847A (https=)
ES (1) ES2923298T3 (https=)
IL (1) IL277278A (https=)
MA (1) MA52012A (https=)
MX (1) MX2020009587A (https=)
NI (1) NI202000058A (https=)
PE (1) PE20210412A1 (https=)
PH (1) PH12020551486A1 (https=)
PY (1) PY1919127A (https=)
RU (1) RU2020130048A (https=)
SG (1) SG11202008102VA (https=)
TW (1) TWI741268B (https=)
UY (1) UY38145A (https=)
WO (1) WO2019175776A1 (https=)

Families Citing this family (9)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US10966999B2 (en) 2017-12-20 2021-04-06 Institute Of Organic Chemistry And Biochemistry Ascr, V.V.I. 3′3′ cyclic dinucleotides with phosphonate bond activating the sting adaptor protein
CN111511754B (zh) 2017-12-20 2023-09-12 捷克共和国有机化学与生物化学研究所 活化sting转接蛋白的具有膦酸酯键的2’3’环状二核苷酸
US10538542B2 (en) * 2018-03-15 2020-01-21 Pfizer Inc. Cyclopentane-based modulators of STING (stimulator of interferon genes)
TWI833744B (zh) 2018-04-06 2024-03-01 捷克科學院有機化學與生物化學研究所 3'3'-環二核苷酸
TW202028179A (zh) 2018-10-08 2020-08-01 美商普萊恩醫療公司 胺基酸化合物及使用方法
JP2022550297A (ja) * 2019-09-25 2022-12-01 ファイザー・インク Sting(インターフェロン遺伝子刺激因子)のヘテロ多環式モジュレーター
WO2021206158A1 (ja) 2020-04-10 2021-10-14 小野薬品工業株式会社 がん治療方法
JP2023553069A (ja) * 2020-12-08 2023-12-20 エフ. ホフマン-ラ ロシュ アーゲー ホスホロジチオエートオリゴヌクレオチドの新規合成
US11964978B2 (en) * 2021-03-18 2024-04-23 Pfizer Inc. Modulators of STING (stimulator of interferon genes)

Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN106459131A (zh) * 2014-06-04 2017-02-22 葛兰素史克知识产权开发有限公司 作为sting调节剂的环状二核苷酸
CN107108684A (zh) * 2015-01-29 2017-08-29 葛兰素史克知识产权开发有限公司 尤其用于治疗癌症的环状二核苷酸

Family Cites Families (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
KR0166088B1 (ko) 1990-01-23 1999-01-15 . 수용해도가 증가된 시클로덱스트린 유도체 및 이의 용도
US5376645A (en) 1990-01-23 1994-12-27 University Of Kansas Derivatives of cyclodextrins exhibiting enhanced aqueous solubility and the use thereof
GB9711643D0 (en) 1997-06-05 1997-07-30 Janssen Pharmaceutica Nv Glass thermoplastic systems
US10538542B2 (en) * 2018-03-15 2020-01-21 Pfizer Inc. Cyclopentane-based modulators of STING (stimulator of interferon genes)

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN106459131A (zh) * 2014-06-04 2017-02-22 葛兰素史克知识产权开发有限公司 作为sting调节剂的环状二核苷酸
CN107108684A (zh) * 2015-01-29 2017-08-29 葛兰素史克知识产权开发有限公司 尤其用于治疗癌症的环状二核苷酸

Also Published As

Publication number Publication date
ES2923298T3 (es) 2022-09-26
UY38145A (es) 2019-10-31
US20190284216A1 (en) 2019-09-19
DOP2020000160A (es) 2020-09-30
CL2020002352A1 (es) 2020-12-18
NI202000058A (es) 2021-01-08
PH12020551486A1 (en) 2021-08-23
JP2021518335A (ja) 2021-08-02
IL277278A (en) 2020-10-29
BR112020018593A2 (pt) 2020-12-29
CA3093631C (en) 2023-01-24
TW201945036A (zh) 2019-12-01
US20200102334A1 (en) 2020-04-02
AU2019234043A1 (en) 2020-09-17
EP3765474A1 (en) 2021-01-20
PE20210412A1 (es) 2021-03-04
KR20200131878A (ko) 2020-11-24
MX2020009587A (es) 2020-10-05
US20230382932A1 (en) 2023-11-30
RU2020130048A3 (https=) 2022-04-15
SG11202008102VA (en) 2020-09-29
RU2020130048A (ru) 2022-04-15
US10968242B2 (en) 2021-04-06
CA3093631A1 (en) 2019-09-19
WO2019175776A1 (en) 2019-09-19
PY1919127A (es) 2020-08-26
US10538542B2 (en) 2020-01-21
EP3765474B1 (en) 2022-06-15
JP7266942B2 (ja) 2023-05-01
US20210230196A1 (en) 2021-07-29
ECSP20057847A (es) 2021-04-29
CR20200382A (es) 2020-12-10
MA52012A (fr) 2021-01-20
TWI741268B (zh) 2021-10-01

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