WO2017123669A1 - Cyclic dinucleotides for treating conditions associated with sting activity such as cancer - Google Patents

Cyclic dinucleotides for treating conditions associated with sting activity such as cancer Download PDF

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Publication number
WO2017123669A1
WO2017123669A1 PCT/US2017/013066 US2017013066W WO2017123669A1 WO 2017123669 A1 WO2017123669 A1 WO 2017123669A1 US 2017013066 W US2017013066 W US 2017013066W WO 2017123669 A1 WO2017123669 A1 WO 2017123669A1
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WIPO (PCT)
Prior art keywords
compound
alkyl
independently selected
group
formula
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Ceased
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PCT/US2017/013066
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English (en)
French (fr)
Inventor
Gary Glick
Shomir Ghosh
Edward James Olhava
William R. Roush
Roger Jones
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Individual
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Individual
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Publication date
Priority to CA3011528A priority Critical patent/CA3011528A1/en
Priority to ES17704338T priority patent/ES3046957T3/es
Priority to KR1020257010190A priority patent/KR20250049441A/ko
Priority to EA201891565A priority patent/EA036421B1/ru
Priority to RS20250892A priority patent/RS67188B1/sr
Priority to EP17704338.7A priority patent/EP3402801B1/en
Priority to DK17704338.7T priority patent/DK3402801T3/da
Priority to SM20250412T priority patent/SMT202500412T1/it
Priority to CN201780015198.2A priority patent/CN109451740B/zh
Priority to HRP20251050TT priority patent/HRP20251050T1/hr
Priority to PL17704338.7T priority patent/PL3402801T3/pl
Priority to AU2017207757A priority patent/AU2017207757B2/en
Priority to FIEP17704338.7T priority patent/FI3402801T3/fi
Priority to JP2018536116A priority patent/JP6867395B2/ja
Priority to KR1020187022863A priority patent/KR102789862B1/ko
Application filed by Individual filed Critical Individual
Priority to LTEPPCT/US2017/013066T priority patent/LT3402801T/lt
Priority to BR112018013808-8A priority patent/BR112018013808A2/pt
Priority to MX2018008266A priority patent/MX2018008266A/es
Priority to NZ745066A priority patent/NZ745066B2/en
Priority to SI201731621T priority patent/SI3402801T1/sl
Priority to MYPI2018702369A priority patent/MY194058A/en
Priority to SG11201805888SA priority patent/SG11201805888SA/en
Priority to US15/748,685 priority patent/US10604542B2/en
Publication of WO2017123669A1 publication Critical patent/WO2017123669A1/en
Priority to IL260427A priority patent/IL260427B/en
Anticipated expiration legal-status Critical
Priority to CONC2018/0008196A priority patent/CO2018008196A2/es
Priority to US16/778,281 priority patent/US10961270B2/en
Priority to US17/160,578 priority patent/US11505571B2/en
Ceased legal-status Critical Current

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Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07H—SUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
    • C07H21/00—Compounds containing two or more mononucleotide units having separate phosphate or polyphosphate groups linked by saccharide radicals of nucleoside groups, e.g. nucleic acids
    • 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
    • A61K31/70—Carbohydrates; Sugars; Derivatives thereof
    • A61K31/7084—Compounds having two nucleosides or nucleotides, e.g. nicotinamide-adenine dinucleotide, flavine-adenine dinucleotide
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K39/00—Medicinal preparations containing antigens or antibodies
    • A61K39/395—Antibodies; Immunoglobulins; Immune serum, e.g. antilymphocytic serum
    • A61K39/39533—Antibodies; Immunoglobulins; Immune serum, e.g. antilymphocytic serum against materials from animals
    • A61K39/3955—Antibodies; Immunoglobulins; Immune serum, e.g. antilymphocytic serum against materials from animals against proteinaceous materials, e.g. enzymes, hormones, lymphokines
    • 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
    • A61P35/00—Antineoplastic agents
    • A61P35/02—Antineoplastic agents specific for leukemia
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07H—SUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
    • C07H21/00—Compounds containing two or more mononucleotide units having separate phosphate or polyphosphate groups linked by saccharide radicals of nucleoside groups, e.g. nucleic acids
    • C07H21/02—Compounds containing two or more mononucleotide units having separate phosphate or polyphosphate groups linked by saccharide radicals of nucleoside groups, e.g. nucleic acids with ribosyl as saccharide radical
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K16/00—Immunoglobulins [IGs], e.g. monoclonal or polyclonal antibodies
    • C07K16/18—Immunoglobulins [IGs], e.g. monoclonal or polyclonal antibodies against material from animals or humans
    • C07K16/28—Immunoglobulins [IGs], e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants
    • C07K16/2803—Immunoglobulins [IGs], e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants against the immunoglobulin superfamily
    • C07K16/2818—Immunoglobulins [IGs], e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants against the immunoglobulin superfamily against CD28 or CD152
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K39/00—Medicinal preparations containing antigens or antibodies
    • A61K2039/505—Medicinal preparations containing antigens or antibodies comprising antibodies

Definitions

  • methods of treatment of a disease in which repressed or impaired STING signaling contributes to the pathology and/or symptoms and/or progression of the disease include administering to a subject in need of such treatment an effective amount of a chemical entity described herein (e.g., a compound described generically or specifically herein or a pharmaceutically acceptable salt thereof or compositions containing the same).
  • a chemical entity described herein e.g., a compound described generically or specifically herein or a pharmaceutically acceptable salt thereof or compositions containing the same.
  • the term“STING” is meant to include, without limitation, nucleic acids, polynucleotides, oligonucleotides, sense and antisense polynucleotide strands, complementary sequences, peptides, polypeptides, proteins, homologous and/or orthologous STING molecules, isoforms, precursors, mutants, variants, derivatives, splice variants, alleles, different species, and active fragments thereof.
  • the term“acceptable” with respect to a formulation, composition or ingredient, as used herein, means having no persistent detrimental effect on the general health of the subject being treated.
  • R’ and R’’ are each independently selected from H and C1-4 alkyl
  • each occurrence of R b1 and R c1 or each occurrence of R c1 is independently selected from the group consisting of: H; C1-6 (e.g., C1- 4) alkyl; -SO2(C1-6 alkyl); -C(O)H; -C(O)(C1-6 alkyl); -C(O)NRR’, wherein R and R’ are each independently selected from H and C1-4 alkyl; and -C(O)O(C1-6 alkyl).
  • X 1 is–OH.
  • X 1 is -OH, -OR a1 , -SH, -SR a1 , -OC(O)H, -OC(O)R a1 , or - OC(O)NR b1 R c1 .
  • X 1 can be -OH, -OR a1 , -OC(O)H, -OC(O)R a1 , or - OC(O)NR b1 R c1 ; e.g., X 1 can be -OH or -OR a1 (e.g., -OH).
  • X 5 is–F, -OH, -OR a1 , -OC(O)H, -OC(O)R a1 , or - OC(O)NR b1 R c1 .
  • X 5 can be–F, -OH, or -OR a1 (e.g., R a1 can be C1-10 alkyl, e.g., C1-4 alkyl).
  • X 5 can be–F or -OH.
  • X 5 can be C1-4 alkyl, C1-4 haloalkyl (e.g., CF3), halo (e.g., F), -CN, or -S(O)2R a1 .
  • X 5 can be C1-4 alkyl, C1-4 haloalkyl (e.g., CF3), or halo (e.g., F).
  • X 5 can be halo (e.g.,–F).
  • X 1 and X 5 are each an independently selected halo (e.g.,– F).
  • Each occurrence of R b1 and R c1 or each occurrence of R c1 can be independently selected from the group consisting of: H; C1-6 (e.g., C1-4) alkyl; -SO2(C1-6 alkyl); -C(O)H; -C(O)(C1-6 alkyl); -C(O)NRR’, wherein R’ and R’’ are each independently selected from H and C1-4 alkyl; and -C(O)O(C1-6 alkyl).
  • [F] In some embodiments of formula (II), (II-A), (III), or (IV):
  • X 1 and X 5 can each be independently selected from the group consisting of H and halo (e.g., F); or X 1 and X 5 can each be an independently selected halo (e.g., F).
  • X 1 and X 5 can each be independently selected from the group consisting of -OH, or -OR a1 (e.g., R a1 can be C1-10 alkyl, e.g., C1-4 alkyl); e.g., X 1 and X 5 can each be -OH.
  • R a1 can be C1-10 alkyl, e.g., C1-4 alkyl
  • X 1 and X 5 can each be -OH.
  • Two of X 2 , X 3 , X 4 and X 6 can be N-R 3 (e.g., N-H), and the others can be O.
  • Y 1 and Y 2 can each be O-; or Y 1 and Y 2 can each be SH or S-.
  • X 1 and X 5 can each be independently selected from the group consisting of H, C1-4 alkyl, C 1-4 haloalkyl (e.g., CF 3 ), halo (e.g., F), -CN, and -S(O) 2 R a1 (in certain embodiments, each of X 1 and X 5 is other than H; e.g.., X 1 and X 5 can each be independently selected from the group consisting of C1-4 alkyl, C1-4 haloalkyl (e.g., CF3), halo (e.g., F), -CN, and - S(O)2R a1 ).
  • a taxane includes, but is not limited, to Taxol, Paclitaxel and/or Docetaxel.
  • a plant alkaloid or terpernoid is a synthetic, semisynthetic or derivative.
  • a podophyllotoxin is, without limitation, an etoposide and/or teniposide.
  • a taxane is, without limitation, docetaxel and/or ortataxel.
  • a cancer therapeutic is a topoisomerase. Topoisomerases are essential enzymes that maintain the topology of DNA.
  • DCA dichloroacetic acid
  • Scheme 4 depicts an example synthesis of cyclic dinucleotide phosphoramidates as disclosed herein that include an amino linkage bonded to the 5’ position of each ribose moiety.
  • reaction suspension changed to a clear solution. After total 3 days, the reaction solution was quenched by the addition of methanol (100 mL). The mixture was concentrated under reduced pressure. The residue was added to a mixture of chloroform (1.5 L) and diethyl ether (4 L) and vigorous stirring for 2 hours. The resulting precipitate was filtered and the filter cake was collected and dried in the air to give crude product. The crude product was added water (3 L) and vigorous stirring for 1 hour.
  • N-(9-((2R,3R,4R,5R)-3-fluoro-4-hydroxy-5-((tritylamino)methyl)tetrahydrofuran-2-yl)- 9H-purin-6-yl)benzamide (INT-E): To a solution of N-(9-((2R,3R,4R,5R)-5- (aminomethyl)-3-fluoro-4-hydroxytetrahydrofuran-2-yl)-9H-purin-6-yl)benzamide (130, 3.0 g, 8.1 mmol) in pyridine (30 mL) was added triethylamine (1.2 g, 12.1 mmol) and triphenylmethyl chloride (2.4 g, 8.6 mmol).

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Organic Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Molecular Biology (AREA)
  • Medicinal Chemistry (AREA)
  • Biochemistry (AREA)
  • Immunology (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Engineering & Computer Science (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Genetics & Genomics (AREA)
  • Biotechnology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Epidemiology (AREA)
  • Mycology (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Endocrinology (AREA)
  • Microbiology (AREA)
  • Biophysics (AREA)
  • Hematology (AREA)
  • Oncology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Saccharide Compounds (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
PCT/US2017/013066 2016-01-11 2017-01-11 Cyclic dinucleotides for treating conditions associated with sting activity such as cancer Ceased WO2017123669A1 (en)

Priority Applications (27)

Application Number Priority Date Filing Date Title
KR1020187022863A KR102789862B1 (ko) 2016-01-11 2017-01-11 Sting 활성과 연관된 상태 예컨대 암의 치료를 위한 시클릭 디뉴클레오티드
KR1020257010190A KR20250049441A (ko) 2016-01-11 2017-01-11 Sting 활성과 연관된 상태 예컨대 암의 치료를 위한 시클릭 디뉴클레오티드
EA201891565A EA036421B1 (ru) 2016-01-11 2017-01-11 Соединения и композиции для лечения состояний, ассоциированных с активностью sting
RS20250892A RS67188B1 (sr) 2016-01-11 2017-01-11 Ciklični dinukleotidi za lečenje stanja povezanih sa aktivnošću sting kao što je kancer
EP17704338.7A EP3402801B1 (en) 2016-01-11 2017-01-11 Cyclic dinucleotides for treating conditions associated with sting activity such as cancer
DK17704338.7T DK3402801T3 (da) 2016-01-11 2017-01-11 Cykliske dinukleotider til behandling af tilstande associeret med sting-aktivitet såsom kræft
SM20250412T SMT202500412T1 (it) 2016-01-11 2017-01-11 Dinucleotidi ciclici per il trattamento di condizioni associate all’attività di sting quali il cancro
CN201780015198.2A CN109451740B (zh) 2016-01-11 2017-01-11 用于治疗与sting活性相关的病症诸如癌症的环状二核苷酸
HRP20251050TT HRP20251050T1 (hr) 2016-01-11 2017-01-11 Ciklični dinukleotidi za liječenje stanja povezanih s aktivnošću sting kao što je rak
PL17704338.7T PL3402801T3 (pl) 2016-01-11 2017-01-11 Cykliczne dinukleotydy do leczenia stanów związanych z działaniem stymulatora genów interferonu (sting), takich jak rak
AU2017207757A AU2017207757B2 (en) 2016-01-11 2017-01-11 Cyclic dinucleotides for treating conditions associated with STING activity such as cancer
FIEP17704338.7T FI3402801T3 (fi) 2016-01-11 2017-01-11 Syklisiä dinukleotideja sting-aktiivisuuteen liittyvien sairauksien kuten syövän hoitamiseksi
JP2018536116A JP6867395B2 (ja) 2016-01-11 2017-01-11 Ｓｔｉｎｇ活性と関連のある症状、例えば癌を治療するための環状ジヌクレオチド
CA3011528A CA3011528A1 (en) 2016-01-11 2017-01-11 Cyclic dinucleotides for treating conditions associated with sting activity such as cancer
MX2018008266A MX2018008266A (es) 2016-01-11 2017-01-11 Dinucleotidos ciclicos para tratar condiciones asociadas con actividad del estimulador de genes del interferon (sting) tales como cancer.
ES17704338T ES3046957T3 (en) 2016-01-11 2017-01-11 Cyclic dinucleotides for treating conditions associated with sting activity such as cancer
BR112018013808-8A BR112018013808A2 (pt) 2016-01-11 2017-01-11 dinucleotídeos cíclicos para o tratamento de condições associadas à atividade de sting, tal como câncer
LTEPPCT/US2017/013066T LT3402801T (lt) 2016-01-11 2017-01-11 Cikliniai dinukleotidai, skirti būklių, susijusių su sting aktyvumu, tokių kaip vėžys, gydymui
NZ745066A NZ745066B2 (en) 2017-01-11 Cyclic dinucleotides for treating conditions associated with sting activity such as cancer
SI201731621T SI3402801T1 (sl) 2016-01-11 2017-01-11 Ciklični dinukleotidi za zdravljenje stanj, povezanih z aktivnostjo sting, kot je rak
MYPI2018702369A MY194058A (en) 2016-01-11 2017-01-11 Cyclic dinucleotides for treating conditions associated with sting activity such as cancer
SG11201805888SA SG11201805888SA (en) 2016-01-11 2017-01-11 Cyclic dinucleotides for treating conditions associated with sting activity such as cancer
US15/748,685 US10604542B2 (en) 2016-01-11 2017-01-11 Cyclic dinucleotides for treating conditions associated with sting activity such as cancer
IL260427A IL260427B (en) 2016-01-11 2018-07-04 Circular dinucleotides for the treatment of conditions related to sting activity such as cancer
CONC2018/0008196A CO2018008196A2 (es) 2016-01-11 2018-08-02 Dinucleótidos cíclicos para tratar condiciones asociadas con actividad del estimulador de genes del interferón (sting) tales como cáncer
US16/778,281 US10961270B2 (en) 2016-01-11 2020-01-31 Compounds and compositions for treating conditions associated with sting activity
US17/160,578 US11505571B2 (en) 2016-01-11 2021-01-28 Compounds and compositions for treating conditions associated with sting activity

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
US201662277273P 2016-01-11 2016-01-11
US62/277,273 2016-01-11
US201662436759P 2016-12-20 2016-12-20
US62/436,759 2016-12-20

Related Child Applications (2)

Application Number Title Priority Date Filing Date
US15/748,685 A-371-Of-International US10604542B2 (en) 2016-01-11 2017-01-11 Cyclic dinucleotides for treating conditions associated with sting activity such as cancer
US16/778,281 Continuation US10961270B2 (en) 2016-01-11 2020-01-31 Compounds and compositions for treating conditions associated with sting activity

Publications (1)

Publication Number Publication Date
WO2017123669A1 true WO2017123669A1 (en) 2017-07-20

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Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/US2017/013066 Ceased WO2017123669A1 (en) 2016-01-11 2017-01-11 Cyclic dinucleotides for treating conditions associated with sting activity such as cancer

Country Status (27)

Country Link
US (3) US10604542B2 (enExample)
EP (1) EP3402801B1 (enExample)
JP (1) JP6867395B2 (enExample)
KR (2) KR20250049441A (enExample)
CN (1) CN109451740B (enExample)
AU (1) AU2017207757B2 (enExample)
BR (1) BR112018013808A2 (enExample)
CA (1) CA3011528A1 (enExample)
CL (1) CL2018001870A1 (enExample)
CO (1) CO2018008196A2 (enExample)
DK (1) DK3402801T3 (enExample)
EA (1) EA036421B1 (enExample)
ES (1) ES3046957T3 (enExample)
FI (1) FI3402801T3 (enExample)
HR (1) HRP20251050T1 (enExample)
IL (1) IL260427B (enExample)
LT (1) LT3402801T (enExample)
MX (1) MX2018008266A (enExample)
MY (1) MY194058A (enExample)
PE (1) PE20181330A1 (enExample)
PL (1) PL3402801T3 (enExample)
PT (1) PT3402801T (enExample)
RS (1) RS67188B1 (enExample)
SG (1) SG11201805888SA (enExample)
SI (1) SI3402801T1 (enExample)
SM (1) SMT202500412T1 (enExample)
WO (1) WO2017123669A1 (enExample)

Cited By (63)

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WO2018190719A2 (en) 2017-04-13 2018-10-18 Aduro Biotech Holdings, Europe B.V. Anti-sirp alpha antibodies
US10106574B2 (en) 2015-08-13 2018-10-23 Merck Sharp & Dohme Corp. Cyclic di-nucleotide compounds as sting agonists
WO2019043634A2 (en) 2017-08-30 2019-03-07 Beijing Xuanyi Pharmasciences Co., Ltd. CYCLIC DI-NUCLEOTIDES AS STIMULATORS OF INTERFERON GENE MODULATORS
WO2019053659A1 (en) * 2017-09-14 2019-03-21 Alios Biopharma, Inc. PHOSPHORAMIDITES OF MODIFIED NUCLEOSIDES
US10246480B2 (en) 2017-02-17 2019-04-02 Eisai R&D Management Co., Ltd. Compounds for the treatment of cancer
WO2019084060A1 (en) 2017-10-24 2019-05-02 Silverback Therapeutics, Inc. CONJUGATES AND METHODS OF USE FOR THE SELECTIVE DELIVERY OF IMMUNOMODULATORY AGENTS
WO2019092660A1 (en) 2017-11-10 2019-05-16 Takeda Pharmaceutical Company Limited Sting modulator compounds, and methods of making and using
EP3505527A1 (en) * 2017-12-29 2019-07-03 Invivogen Cyclic dinucleotides for cytokine induction
WO2019160884A1 (en) * 2018-02-13 2019-08-22 Bristol-Myers Squibb Company Cyclic dinucleotides as anticancer agents
US10414747B2 (en) 2016-10-04 2019-09-17 Merck Sharp & Dohme Corp. Benzo[b]thiophene compounds as sting agonists
US10413612B2 (en) 2016-08-30 2019-09-17 Dana-Farber Cancer Institute, Inc. Method of treating cancer with a biomaterial and a toll-like receptor agonist
WO2019180683A1 (en) 2018-03-23 2019-09-26 Takeda Pharmaceutical Company Limited Sting modulator compounds with sulfamate linkages, and methods of making and using
US10449211B2 (en) 2015-03-10 2019-10-22 Aduro Biotech, Inc. Compositions and methods for activating “stimulator of interferon gene”—dependent signalling
US10519188B2 (en) 2016-03-18 2019-12-31 Immunesensor Therapeutics, Inc. Cyclic di-nucleotide compounds and methods of use
WO2020050406A1 (ja) 2018-09-06 2020-03-12 第一三共株式会社 新規環状ジヌクレオチド誘導体及びその抗体薬物コンジュゲート
WO2020056008A1 (en) 2018-09-12 2020-03-19 Silverback Therapeutics, Inc. Compositions for the treatment of disease with immune stimulatory conjugates
WO2020057546A1 (zh) 2018-09-21 2020-03-26 上海迪诺医药科技有限公司 环状二核苷酸类似物、其药物组合物及应用
KR20200039796A (ko) * 2017-08-31 2020-04-16 브리스톨-마이어스 스큅 컴퍼니 항암제로서의 시클릭 디뉴클레오티드
WO2020089815A1 (en) 2018-10-31 2020-05-07 Novartis Ag Antibody conjugates comprising sting agonist
WO2020117739A1 (en) * 2018-12-04 2020-06-11 Bristol-Myers Squibb Company Process for the preparation of a cyclic dinucleotide
WO2020163415A1 (en) * 2019-02-05 2020-08-13 Bristol-Myers Squibb Company Synthesis of 1,2,5-tri-0-benz0yl-3-dibenzylamin0-3-de0xyrib0se as intermediate for producing 3'-amino-3'-deoxyadenosine and 3'-amino-3'-deoxyguanosine and the protected derivatives thereof
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