[go: up one dir, main page]

PE20190705A1 - COMPUESTOS DE BENZO[b] TIOFENO COMO AGONISTAS DE STING - Google Patents

COMPUESTOS DE BENZO[b] TIOFENO COMO AGONISTAS DE STING

Info

Publication number
PE20190705A1
PE20190705A1 PE2019000764A PE2019000764A PE20190705A1 PE 20190705 A1 PE20190705 A1 PE 20190705A1 PE 2019000764 A PE2019000764 A PE 2019000764A PE 2019000764 A PE2019000764 A PE 2019000764A PE 20190705 A1 PE20190705 A1 PE 20190705A1
Authority
PE
Peru
Prior art keywords
thiophen
sting agonists
compounds
benzo compounds
haloalkyl
Prior art date
Application number
PE2019000764A
Other languages
English (en)
Inventor
Michael D Altman
Brandon D Cash
Wonsuk Chang
Jared N Cumming
Andrew M Haidle
Timothy J Henderson
James P Jewell
Matthew A Larsen
Rui Liang
Jongwon Lim
Min Lu
Ryan D Otte
Tony Siu
Benjamin Wesley Trotter
Sriram Tyagarajan
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 PE20190705A1 publication Critical patent/PE20190705A1/es

Links

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)
  • 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

Se refiere a un compuesto de formula (Ia') o su sal farmaceuticamente aceptable, donde: R1 es H, halogeno, entre otros; R2 es H, CN, entre otros; R3 es H, COOR6, entre otros; R4 es H, OR6, entre otros; R5 es H, N(R6)2, entre otros; R6 es H, alquilo C1-C6, y haloalquilo C1-C6, pudiendo estar los 2 ultimos sustituidos con OH, O(alquilo C1-C3), y O(haloalquilo C1-C3); X1 es C(O); X2 es (C(R8)2)(1-3); R8 es H, CN, entre otros; y X3 es C(S)OR6, SO2R6, entre otros. Tambien se refiere a composiciones farmaceuticas que comprenden al compuesto de la invencion y a metodos de preparacion. Dichos compuestos son agonistas de STING (estimulador de genes de interferon) y son utiles en el tratamiento de enfermedades como el cancer
PE2019000764A 2016-10-04 2017-10-02 COMPUESTOS DE BENZO[b] TIOFENO COMO AGONISTAS DE STING PE20190705A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US201662404062P 2016-10-04 2016-10-04

Publications (1)

Publication Number Publication Date
PE20190705A1 true PE20190705A1 (es) 2019-05-17

Family

ID=60084122

Family Applications (1)

Application Number Title Priority Date Filing Date
PE2019000764A PE20190705A1 (es) 2016-10-04 2017-10-02 COMPUESTOS DE BENZO[b] TIOFENO COMO AGONISTAS DE STING

Country Status (39)

Country Link
US (3) US10414747B2 (es)
EP (1) EP3523287B1 (es)
JP (1) JP6636673B2 (es)
KR (1) KR102312721B1 (es)
CN (1) CN110036001B (es)
AR (1) AR109788A1 (es)
AU (1) AU2017339418C1 (es)
CA (1) CA3038903C (es)
CL (1) CL2019000902A1 (es)
CO (1) CO2019003349A2 (es)
CR (1) CR20190168A (es)
CY (1) CY1124837T1 (es)
DK (1) DK3523287T3 (es)
DO (1) DOP2019000083A (es)
EA (1) EA037626B1 (es)
EC (1) ECSP19026680A (es)
ES (1) ES2893532T3 (es)
GE (2) GEAP202115066A (es)
HR (1) HRP20211617T1 (es)
HU (1) HUE056502T2 (es)
IL (1) IL265678B2 (es)
JO (1) JOP20190070B1 (es)
LT (1) LT3523287T (es)
MA (1) MA46452B1 (es)
MD (1) MD3523287T2 (es)
MX (1) MX386187B (es)
MY (1) MY196383A (es)
NI (1) NI201900029A (es)
PE (1) PE20190705A1 (es)
PH (1) PH12019500712B1 (es)
PL (1) PL3523287T3 (es)
PT (1) PT3523287T (es)
RS (1) RS62410B1 (es)
SG (1) SG10202008647TA (es)
SI (1) SI3523287T1 (es)
TN (2) TN2020000159A1 (es)
TW (1) TWI796306B (es)
UA (1) UA125223C2 (es)
WO (1) WO2018067423A1 (es)

Families Citing this family (101)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
HUE060396T2 (hu) 2016-03-18 2023-02-28 Immune Sensor Llc Ciklikus DI-nukleotid vegyületek és azok felhasználási módszerei
CA3029644A1 (en) 2016-07-06 2018-01-11 Sperovie Biosciences, Inc. Compounds, compositions, and methods for the treatment of disease
GEAP202115066A (en) * 2016-10-04 2021-04-12 Merck Sharp & Dohme BENZO[b]THIOPHENE COMPOUNDS AS STING AGONISTS
IL265921B2 (en) 2016-10-14 2024-05-01 Prec Biosciences Inc Engineered meganucleases specific for recognition sequences in the hepatitis b virus genome
JOP20170192A1 (ar) 2016-12-01 2019-01-30 Takeda Pharmaceuticals Co داي نوكليوتيد حلقي
IL315837A (en) 2017-04-13 2024-11-01 Sairopa B V Anti-SIRP-alpha antibodies
AU2018311965A1 (en) 2017-08-04 2020-02-13 Merck Sharp & Dohme Llc Combinations of PD-1 antagonists and benzo[b]thiophene sting antagonists for cancer treatment
EP3661498A4 (en) * 2017-08-04 2021-04-21 Merck Sharp & Dohme Corp. BENZO [B] THIOPHEN STING ANTAGONISTS FOR CANCER TREATMENT
CA3074232A1 (en) 2017-08-31 2019-03-07 Sperovie Biosciences, Inc. Compounds, compositions, and methods for the treatment of disease
WO2019051489A1 (en) 2017-09-11 2019-03-14 Sperovie Biosciences, Inc. COMPOUNDS, COMPOSITIONS AND METHODS OF TREATING DISEASE
US11584774B2 (en) 2017-09-11 2023-02-21 F-star Therapeutics, Inc. Compounds, compositions, and methods for the treatment of disease
JP7262451B2 (ja) * 2017-10-05 2023-04-21 グラクソスミスクライン、インテレクチュアル、プロパティー、ディベロップメント、リミテッド Ｓｔｉｎｇアゴニストの投与方法
SG11202004113VA (en) 2017-11-10 2020-06-29 Takeda Pharmaceuticals Co Sting modulator compounds, and methods of making and using
MX2020005680A (es) 2017-12-01 2020-08-20 Texas A & M Univ Sys Tratamiento antisentido del sindrome de angelman.
KR102492115B1 (ko) 2017-12-20 2023-01-27 인스티튜트 오브 오가닉 케미스트리 앤드 바이오케미스트리 에이에스 씨알 브이.브이.아이. Sting 어댑터 단백질을 활성화하는 포스포네이트 결합을 가진 2'3' 사이클릭 다이뉴클레오티드
AU2018392213B2 (en) 2017-12-20 2021-03-04 Institute Of Organic Chemistry And Biochemistry Ascr, V.V.I. 3'3' cyclic dinucleotides with phosphonate bond activating the STING adaptor protein
JP7050165B2 (ja) 2018-02-26 2022-04-07 ギリアード サイエンシーズ， インコーポレイテッド Ｈｂｖ複製阻害剤としての置換ピロリジン化合物
TWI793294B (zh) * 2018-04-03 2023-02-21 美商默沙東有限責任公司 Sting促效劑化合物
WO2019195063A1 (en) * 2018-04-03 2019-10-10 Merck Sharp & Dohme Corp. Aza-benzothiophene compounds as sting agonists
WO2019195181A1 (en) 2018-04-05 2019-10-10 Gilead Sciences, Inc. Antibodies and fragments thereof that bind hepatitis b virus protein x
TWI818007B (zh) 2018-04-06 2023-10-11 捷克科學院有機化學與生物化學研究所 2'3'-環二核苷酸
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
TW202005654A (zh) 2018-04-06 2020-02-01 捷克科學院有機化學與生物化學研究所 ２，２，─環二核苷酸
US11142750B2 (en) 2018-04-12 2021-10-12 Precision Biosciences, Inc. Optimized engineered meganucleases having specificity for a recognition sequence in the Hepatitis B virus genome
WO2019211799A1 (en) 2018-05-03 2019-11-07 Institute Of Organic Chemistry And Biochemistry Ascr, V.V.I. 2'3'-cyclic dinucleotide analogue comprising a cyclopentanyl modified nucleotide
GB201807924D0 (en) 2018-05-16 2018-06-27 Ctxt Pty Ltd Compounds
US10947227B2 (en) 2018-05-25 2021-03-16 Incyte Corporation Tricyclic heterocyclic compounds as sting activators
WO2020010451A1 (en) * 2018-07-10 2020-01-16 Trillium Therapeutics Inc. Heteroaromatic-fused imidazolyl amides, compositions and uses thereof as sting agonists
CA3106110A1 (en) 2018-07-10 2020-01-16 Sperovie Biosciences, Inc. Compounds, compositions, and methods for the treatment of disease
KR20210040080A (ko) * 2018-07-26 2021-04-12 브리스톨-마이어스 스큅 컴퍼니 암의 치료를 위한 lag-3 조합 요법
US11008344B2 (en) 2018-07-31 2021-05-18 Incyte Corporation Tricyclic heteroaryl compounds as STING activators
US10875872B2 (en) 2018-07-31 2020-12-29 Incyte Corporation Heteroaryl amide compounds as sting activators
WO2020028097A1 (en) 2018-08-01 2020-02-06 Gilead Sciences, Inc. Solid forms of (r)-11-(methoxymethyl)-12-(3-methoxypropoxy)-3,3-dimethyl-8-0x0-2,3,8,13b-tetrahydro-1h-pyrido[2,1-a]pyrrolo[1,2-c] phthalazine-7-c arboxylic acid
CA3251690A1 (en) 2018-09-06 2025-11-29 Daiichi Sankyo Company, Limited Novel cyclic dinucleotide derivative and antibody-drug conjugate thereof
TWI855000B (zh) 2018-10-11 2024-09-11 日商小野藥品工業股份有限公司 Ｓｔｉｎｇ促效化合物
EP3873608A1 (en) 2018-10-31 2021-09-08 Gilead Sciences, Inc. Substituted 6-azabenzimidazole compounds having hpk1 inhibitory activity
AU2019372046B2 (en) 2018-10-31 2022-05-26 Gilead Sciences, Inc. Substituted 6-azabenzimidazole compounds as HPK1 inhibitors
US11596692B1 (en) 2018-11-21 2023-03-07 Incyte Corporation PD-L1/STING conjugates and methods of use
CN111393404B (zh) * 2019-01-02 2023-02-17 中国科学院上海药物研究所 一类苯并噻吩类化合物及其药物组合物及应用
CN111393405B (zh) 2019-01-02 2022-11-25 中国科学院上海药物研究所 一类含氟取代的苯并噻吩类化合物及其药物组合物及应用
WO2020146237A1 (en) 2019-01-07 2020-07-16 Incyte Corporation Heteroaryl amide compounds as sting activators
WO2020165600A1 (en) 2019-02-14 2020-08-20 Bicycletx Limited Bicyclic peptide ligand sting conjugates and uses thereof
US12318403B2 (en) 2019-03-07 2025-06-03 Institute Of Organic Chemistry And Biochemistry Ascr, V.V.I. 2′3′-cyclic dinucleotides and prodrugs thereof
EP3935065A1 (en) 2019-03-07 2022-01-12 Institute of Organic Chemistry and Biochemistry ASCR, V.V.I. 3'3'-cyclic dinucleotide analogue comprising a cyclopentanyl modified nucleotide as sting modulator
JP7350872B2 (ja) 2019-03-07 2023-09-26 インスティチュート オブ オーガニック ケミストリー アンド バイオケミストリー エーエスシーアール，ヴイ．ヴイ．アイ． ３’３’－環状ジヌクレオチドおよびそのプロドラッグ
TWI751517B (zh) 2019-04-17 2022-01-01 美商基利科學股份有限公司 類鐸受體調節劑之固體形式
TWI751516B (zh) 2019-04-17 2022-01-01 美商基利科學股份有限公司 類鐸受體調節劑之固體形式
CN111848573B (zh) * 2019-04-30 2023-04-07 四川科伦博泰生物医药股份有限公司 苯并噻吩酰胺类化合物及其制备方法和用途
CN111848572B (zh) * 2019-04-30 2023-03-31 四川科伦博泰生物医药股份有限公司 酰胺类化合物及其制备方法和用途
WO2020221038A1 (zh) 2019-04-30 2020-11-05 四川科伦博泰生物医药股份有限公司 苯并噻吩类化合物及其制备方法和用途
EP3962493A2 (en) 2019-05-03 2022-03-09 Flagship Pioneering Innovations V, Inc. Methods of modulating immune activity/level of irf or sting or of treating cancer, comprising the administration of a sting modulator and/or purinergic receptor modulator or postcellular signaling factor
WO2020237025A1 (en) 2019-05-23 2020-11-26 Gilead Sciences, Inc. Substituted exo-methylene-oxindoles which are hpk1/map4k1 inhibitors
MX2021015452A (es) 2019-06-25 2022-02-11 Gilead Sciences Inc Proteinas de fusion flt3l-fc y metodos de uso.
JP7622031B2 (ja) 2019-07-05 2025-01-27 タンボ・インコーポレイテッド トランス－シクロオクテン生体直交型薬剤並びに癌及び免疫療法における使用
GB201910305D0 (en) 2019-07-18 2019-09-04 Ctxt Pty Ltd Compounds
GB201910304D0 (en) 2019-07-18 2019-09-04 Ctxt Pty Ltd Compounds
CA3149482A1 (en) 2019-08-02 2021-02-11 Mersana Therapeutics, Inc. 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
WO2021034804A1 (en) 2019-08-19 2021-02-25 Gilead Sciences, Inc. Pharmaceutical formulations of tenofovir alafenamide
KR102821711B1 (ko) * 2019-08-21 2025-06-16 더 스크립스 리서치 인스티튜트 인터페론 유전자의 자극인자 sting의 비시클릭 효능제
US20220288065A1 (en) * 2019-08-21 2022-09-15 The Scripps Research Institute Monocyclic agonists of stimulator of interferon genes sting
KR20220074917A (ko) 2019-09-30 2022-06-03 길리애드 사이언시즈, 인코포레이티드 Hbv 백신 및 hbv를 치료하는 방법
WO2021083060A1 (zh) * 2019-10-28 2021-05-06 中国科学院上海药物研究所 五元杂环氧代羧酸类化合物及其医药用途
CN116057068A (zh) 2019-12-06 2023-05-02 精密生物科学公司 对乙型肝炎病毒基因组中的识别序列具有特异性的优化的工程化大范围核酸酶
EP4069683A1 (en) * 2019-12-06 2022-10-12 Mersana Therapeutics, Inc. Dimeric compounds as sting agonists
CA3164751A1 (en) 2019-12-18 2021-06-24 Benjamin Joseph MORROW Compounds
JPWO2021177438A1 (es) 2020-03-06 2021-09-10
AU2021237718B2 (en) 2020-03-20 2023-09-21 Gilead Sciences, Inc. Prodrugs of 4'-C-substituted-2-halo-2'-deoxyadenosine nucleosides and methods of making and using the same
CA3174297A1 (en) 2020-04-02 2021-10-07 Jeremy R. Duvall Antibody drug conjugates comprising sting agonists
WO2021205631A1 (ja) 2020-04-10 2021-10-14 小野薬品工業株式会社 Ｓｔｉｎｇ作動化合物
KR20220167275A (ko) 2020-04-10 2022-12-20 오노 야꾸힝 고교 가부시키가이샤 암 치료 방법
US12390537B2 (en) 2020-05-13 2025-08-19 Massachusetts Institute Of Technology Compositions of polymeric microdevices and methods of use thereof in cancer immunotherapy
CN113861161A (zh) * 2020-06-30 2021-12-31 上海海和药物研究开发股份有限公司 一种芳基并芳杂环衍生物及其制备方法和用途
PE20230779A1 (es) 2020-08-07 2023-05-09 Gilead Sciences Inc Profarmacos de analogos de nucleotidos de fosfonamida y su uso farmaceutico
JP2023537066A (ja) 2020-08-07 2023-08-30 タンボ・インコーポレイテッド トランス－シクロオクテン生体直交型薬剤並びに癌及び免疫療法における使用
WO2022050300A1 (ja) 2020-09-02 2022-03-10 第一三共株式会社 新規エンド－β－Ｎ－アセチルグルコサミニダーゼ
EP4240488A1 (en) 2020-11-09 2023-09-13 Takeda Pharmaceutical Company Limited Antibody drug conjugates
CN113429384B (zh) * 2021-05-12 2022-04-08 中山大学附属第五医院 一类干扰素基因刺激因子靶向的放射性pet显像剂
JP2024518558A (ja) 2021-05-13 2024-05-01 ギリアード サイエンシーズ， インコーポレイテッド ＴＬＲ８調節化合物と抗ＨＢＶ ｓｉＲＮＡ治療薬との組合せ
US20220389394A1 (en) 2021-05-18 2022-12-08 Gilead Sciences, Inc. METHODS OF USING FLT3L-Fc FUSION PROTEINS
EP4359413A1 (en) 2021-06-23 2024-05-01 Gilead Sciences, Inc. Diacylglyercol kinase modulating compounds
CN117355531A (zh) 2021-06-23 2024-01-05 吉利德科学公司 二酰基甘油激酶调节化合物
CN117377671A (zh) 2021-06-23 2024-01-09 吉利德科学公司 二酰基甘油激酶调节化合物
CA3220923A1 (en) 2021-06-23 2022-12-29 Gilead Sciences, Inc. Diacylglyercol kinase modulating compounds
WO2023284719A1 (en) * 2021-07-13 2023-01-19 Nanjing University A pt conjugate and the use thereof
CN113429387B (zh) * 2021-07-27 2022-10-28 中国药科大学 一种苯并[b]硒吩类STING调控剂、其制备方法及用途
CN115772154B (zh) * 2021-09-08 2024-04-30 上海交通大学 一类含有氘取代的苯并噻吩类衍生物及其制备与用途
IL315341A (en) 2022-03-02 2024-10-01 Daiichi Sankyo Co Ltd METHOD FOR PRODUCING Fc-CONTAINING MOLECULE
WO2023211940A1 (en) * 2022-04-25 2023-11-02 The Regents Of The University Of Michigan Sting agonists, formulations, and uses thereof
EP4514785A1 (en) * 2022-04-25 2025-03-05 The Regents of The University of Michigan Dual functioning immune modulating compounds, formulations, and uses thereof
EP4582106A1 (en) 2022-08-29 2025-07-09 Daiichi Sankyo Company, Limited Antibody-drug conjugate including mutant fc region
TW202435862A (zh) * 2023-02-24 2024-09-16 大陸商深圳真實生物醫藥科技有限公司 芳基三并環類sting促效劑及其用途
CN116354922B (zh) * 2023-03-31 2025-04-25 药康众拓(江苏)医药科技有限公司 氘代苯并噻吩类化合物及其药物组合物和用途
WO2024211577A1 (en) 2023-04-05 2024-10-10 Massachusetts Institute Of Technology Hybrid polymeric systems and methods of use thereof
WO2025007743A1 (en) * 2023-07-04 2025-01-09 Primelink Biotherapeutics (Shenzhen) Co., Ltd. Sting agonists and uses thereof
WO2025096619A1 (en) * 2023-10-30 2025-05-08 The Regents Of The University Of Michigan Dual functioning immune modulating compounds, formulations, and uses thereof
WO2025096584A1 (en) * 2023-10-30 2025-05-08 The Regents Of The University Of Michigan Sting agonists, compositions, and uses thereof
US20250345390A1 (en) 2024-05-13 2025-11-13 Gilead Sciences, Inc. Combination therapies
US20250345389A1 (en) 2024-05-13 2025-11-13 Gilead Sciences, Inc. Combination therapies
WO2025240242A1 (en) 2024-05-13 2025-11-20 Gilead Sciences, Inc. Combination therapies with ribavirin
WO2025240246A1 (en) 2024-05-13 2025-11-20 Gilead Sciences, Inc. Combination therapies with ribavirin
CN121293183A (zh) * 2025-12-15 2026-01-09 北京悦康科创医药科技股份有限公司 含有苯并噻吩结构用于激活sting通路的佐剂脂质及其组合物

Family Cites Families (76)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB532822A (en) * 1939-08-11 1941-01-31 John David Kendall Improvements in and relating to the production of ª‡-coumarilyl and ª‡-thionaphthenoyl-acetic acid esters
GB1383114A (en) * 1972-06-22 1975-02-05 English Electric Valve Co Ltd Magnetrons
US4342691A (en) 1980-04-28 1982-08-03 American Cyanamid Company ω-Heteroaroyl(propionyl or butyryl)-L-prolines
US4342689A (en) 1980-04-28 1982-08-03 American Cyanamid Company ω-Heteroaroyl(propionyl or butyryl)-L-prolines
US4342690A (en) 1980-04-28 1982-08-03 American Cyanamid Company ω-Heteroaroyl(propionyl or butyryl)-L-prolines
US4299769A (en) * 1980-04-28 1981-11-10 American Cyanamid Company ω-Heteroaroyl(propionyl or butyryl)-L-prolines
EP0146243A1 (en) 1983-10-31 1985-06-26 Merck Frosst Canada Inc. Lipoxygenase inhibitors
DE68924308T2 (de) * 1988-07-11 1996-04-04 Akzo Nobel Nv Pyridazinon-Derivate.
US5559127A (en) 1992-10-14 1996-09-24 Merck & Co., Inc. Fibrinogen receptor antagonists
US5569655A (en) 1993-09-14 1996-10-29 Sterling Winthrop Inc. Substituted heterocyclylisoquinolinium salts and compositions and method of use thereof
WO1999062897A1 (en) 1998-06-03 1999-12-09 Merck & Co., Inc. Hiv integrase inhibitors
US6262055B1 (en) 1998-06-03 2001-07-17 Merck & Co., Inc. HIV integrase inhibitors
PE20010306A1 (es) 1999-07-02 2001-03-29 Agouron Pharma Compuestos de indazol y composiciones farmaceuticas que los contienen utiles para la inhibicion de proteina kinasa
GB0018891D0 (en) 2000-08-01 2000-09-20 Novartis Ag Organic compounds
WO2001070675A2 (en) 2000-03-24 2001-09-27 Methylgene, Inc. Inhibitors of histone deacetylase
US20040175803A1 (en) 2001-02-20 2004-09-09 Jean-Francois Meritet Interferon-alpha induced gene
PT1537878E (pt) 2002-07-03 2010-11-18 Ono Pharmaceutical Co Composições de imunopotenciação
CN101899114A (zh) 2002-12-23 2010-12-01 惠氏公司 抗pd-1抗体及其用途
KR20050107399A (ko) 2003-01-23 2005-11-11 오노 야꾸힝 고교 가부시키가이샤 인간 ｐｄ-1에 대하여 특이성을 갖는 물질
CA2537119A1 (en) 2003-09-02 2005-03-10 Merck & Co., Inc. Ophthalmic compositions for treating ocular hypertension
CA2559802C (en) 2004-03-15 2013-05-21 David K.R. Karaolis Method for stimulating the immune, inflammatory or neuroprotective response
AU2006244885B2 (en) 2005-05-09 2011-03-31 E. R. Squibb & Sons, L.L.C. Human monoclonal antibodies to programmed death 1(PD-1) and methods for treating cancer using anti-PD-1 antibodies alone or in combination with other immunotherapeutics
CN101248089A (zh) 2005-07-01 2008-08-20 米德列斯公司 抗程序性死亡配体1（pd-l1）的人单克隆抗体
EP1782826A1 (en) 2005-11-08 2007-05-09 GBF Gesellschaft für Biotechnologische Forschung mbH PQS and c-diGMP and its conjugates as adjuvants and their uses in pharmaceutical compositions
CA2691357C (en) 2007-06-18 2014-09-23 N.V. Organon Antibodies to human programmed death receptor pd-1
US8168757B2 (en) 2008-03-12 2012-05-01 Merck Sharp & Dohme Corp. PD-1 binding proteins
US20110159023A1 (en) 2008-08-25 2011-06-30 Solomon Langermann Pd-1 antagonists and methods for treating infectious disease
BRPI0919377A2 (pt) 2008-09-26 2016-09-27 Dana Farber Cancer Inst Inc anticorpo isolado ou um fragmento ligante de antígeno do memso, ácido nucleico isolado, vetor, célula hospedeira, composição farmacêutica, método de produzir o referido anticorpo ou fragmento, uso dos mesmos, e composição compreendendo o referido anticorpo ou fragmento
WO2010047774A2 (en) 2008-10-20 2010-04-29 The Texas A & M University System Inhibitors of mycobacterium tuberculosis malate synthase, methods of marking and uses thereof
HUE034832T2 (hu) 2008-12-09 2021-12-28 Hoffmann La Roche Anti-PD-L1 antitestek és alkalmazásuk T-sejt-funkció fokozására
WO2011066342A2 (en) 2009-11-24 2011-06-03 Amplimmune, Inc. Simultaneous inhibition of pd-l1/pd-l2
WO2012068702A1 (zh) * 2010-11-23 2012-05-31 中国医学科学院医药生物技术研究所 苯并五元不饱和杂环类化合物及其制备方法
JP5887947B2 (ja) 2011-03-28 2016-03-16 ソニー株式会社 透明導電膜、ヒータ、タッチパネル、太陽電池、有機ｅｌ装置、液晶装置および電子ペーパ
EP2697242B1 (en) 2011-04-13 2018-10-03 Merck Sharp & Dohme Corp. 2'-azido substituted nucleoside derivatives and methods of use thereof for the treatment of viral diseases
BR112014002353B1 (pt) 2011-08-01 2022-09-27 Genentech, Inc Usos de antagonistas de ligação do eixo pd-1 e inibidores de mek, composições farmacêuticas, e kit
KR20150022996A (ko) 2012-06-08 2015-03-04 아두로 바이오테크 암 면역요법을 위한 조성물 및 방법
CN103840995B (zh) 2012-11-26 2017-10-24 华为技术有限公司 Ip报文处理方法、装置及网络系统
SG10201704611WA (en) 2012-12-13 2017-07-28 Aduro Biotech Inc Compositions comprising cyclic purine dinucleotides having defined stereochemistries and methods for their preparation and use
WO2014099824A1 (en) 2012-12-19 2014-06-26 Board Of Regents, The University Of Texas System Pharmaceutical targeting of a mammalian cyclic di-nucleotide signaling pathway
US9211300B2 (en) 2012-12-19 2015-12-15 Idenix Pharmaceuticals Llc 4′-fluoro nucleosides for the treatment of HCV
EP2970119B1 (en) 2013-03-14 2021-11-03 Merck Sharp & Dohme Corp. Novel indole derivatives useful as anti-diabetic agents
ES2822584T3 (es) 2013-05-03 2021-05-04 Univ California Inducción de dinucleótidos cíclicos del interferón tipo I
WO2014189806A1 (en) 2013-05-18 2014-11-27 Aduro Biotech, Inc. Compositions and methods for inhibiting "stimulator of interferon gene" dependent signalling
US9549944B2 (en) 2013-05-18 2017-01-24 Aduro Biotech, Inc. Compositions and methods for inhibiting “stimulator of interferon gene”—dependent signalling
CA2904536A1 (en) 2013-05-18 2014-11-27 Aduro Biotech, Inc. Compositions and methods for activating "stimulator of interferon gene"-dependent signalling
US10176292B2 (en) 2013-07-31 2019-01-08 Memorial Sloan-Kettering Cancer Center STING crystals and modulators
EP3071209A4 (en) * 2013-11-19 2017-08-16 The University of Chicago Use of sting agonist as cancer treatment
US10092644B2 (en) 2013-11-22 2018-10-09 Brock University Use of fluorinated cyclic dinucleotides as oral vaccine adjuvants
US9315523B2 (en) 2013-12-06 2016-04-19 Rutgers, The State University Of New Jersey Cyclic dinucleosides
WO2015143712A1 (en) 2014-03-28 2015-10-01 Merck Sharp & Dohme Corp. 4'-substituted nucleoside reverse transcriptase inhibitors
WO2015161137A1 (en) 2014-04-16 2015-10-22 Idenix Pharmaceuticals, Inc. 3'-substituted methyl or alkynyl nucleosides for the treatment of hcv
CN103908468B (zh) 2014-04-21 2017-02-08 上海捌加壹医药科技有限公司 环二核苷酸cGAMP在制备抗肿瘤药物中的应用
PE20170198A1 (es) 2014-06-04 2017-04-08 Glaxosmithkline Ip Dev Ltd Dinucleotidos ciclicos como moduladores de sting
WO2015189117A1 (de) 2014-06-12 2015-12-17 Bayer Pharma Aktiengesellschaft Heterobicyclisch substituierte 4-oxobutansäure-derivate und ihre verwendung
WO2016096577A1 (en) 2014-12-16 2016-06-23 Invivogen Combined use of a chemotherapeutic agent and a cyclic dinucleotide for cancer treatment
US10011630B2 (en) 2014-12-16 2018-07-03 Invivogen Cyclic dinucleotides for cytokine induction
CN112626153A (zh) 2014-12-17 2021-04-09 立博美华基因科技有限责任公司 用cGAMP或cGAsMP治疗癌症的方法
GB201501462D0 (en) * 2015-01-29 2015-03-18 Glaxosmithkline Ip Dev Ltd Novel compounds
HK1247089A1 (zh) 2015-03-10 2018-09-21 Aduro Biotech, Inc. 用於活化“干扰素基因刺激物”依赖性信号传导的组合物和方法
WO2017011622A1 (en) 2015-07-14 2017-01-19 Spring Bank Pharmaceuticals, Inc. Compounds and compositions that induce rig-i-and other pattern recongnition receptors
CA3030582A1 (en) 2015-07-22 2017-01-26 The Royal Institution For The Advancement Of Learning/Mcgill University Compounds and uses thereof in the treatment of cancers and other medical conditions
WO2017027645A1 (en) 2015-08-13 2017-02-16 Merck Sharp & Dohme Corp. Cyclic di-nucleotide compounds as sting agonists
US9809597B2 (en) 2015-08-20 2017-11-07 The Board Of Trustees Of The Leland Stanford Junior University Ganciclovir derivatives for modulating innate and adaptive immunity and for use in immunotherapy
BR112018008339A2 (pt) 2015-10-28 2018-10-30 Aduro Biotech Inc composições e métodos para ativar estimulador de sinalização dependente do gene de interferon
HK1250032A1 (zh) 2015-12-03 2018-11-23 Glaxosmithkline Intellectual Property Development Limited 作为sting调节剂的环状嘌呤二核苷酸
DE212016000029U1 (de) 2015-12-07 2017-07-30 Opi Vi - Ip Holdco Llc Zusammensetzungen von Antikörperkonstrukt-Agonist-Konjugaten
SG11201805888SA (en) 2016-01-11 2018-08-30 Innate Tumor Immunity Inc Cyclic dinucleotides for treating conditions associated with sting activity such as cancer
WO2017123657A1 (en) 2016-01-11 2017-07-20 Gary Glick Cyclic dinucleotides for treating conditions associated with sting activity such as cancer
HUE060396T2 (hu) 2016-03-18 2023-02-28 Immune Sensor Llc Ciklikus DI-nukleotid vegyületek és azok felhasználási módszerei
MX387354B (es) 2016-04-07 2025-03-18 Glaxosmithkline Ip Dev Ltd Amidas heterocíclicas útiles como moduladores de proteínas.
CN109563081A (zh) 2016-04-07 2019-04-02 葛兰素史克知识产权开发有限公司 可用作蛋白调节剂的杂环酰胺类
ES2993451T3 (en) 2016-06-13 2024-12-30 Glaxosmithkline Ip Dev Ltd Substituted pyridines as inhibitors of dnmt1
EP3507367A4 (en) 2016-07-05 2020-03-25 Aduro BioTech, Inc. CYCLIC DINUCLEOTID COMPOUNDS WITH INCLUDED NUCLEIC ACIDS AND USES THEREOF
GEAP202115066A (en) * 2016-10-04 2021-04-12 Merck Sharp & Dohme BENZO[b]THIOPHENE COMPOUNDS AS STING AGONISTS
EP3661498A4 (en) * 2017-08-04 2021-04-21 Merck Sharp & Dohme Corp. BENZO [B] THIOPHEN STING ANTAGONISTS FOR CANCER TREATMENT
AU2018311965A1 (en) * 2017-08-04 2020-02-13 Merck Sharp & Dohme Llc Combinations of PD-1 antagonists and benzo[b]thiophene sting antagonists for cancer treatment

Also Published As

Publication number Publication date
CA3038903C (en) 2021-07-27
BR112019006816A2 (pt) 2019-07-30
GEAP202115066A (en) 2021-04-12
IL265678A (en) 2019-05-30
EP3523287B1 (en) 2021-09-01
EA037626B1 (ru) 2021-04-22
MD3523287T2 (ro) 2021-12-31
LT3523287T (lt) 2021-11-10
GEP20217285B (en) 2021-08-10
JOP20190070A1 (ar) 2019-04-04
US10414747B2 (en) 2019-09-17
US20180093964A1 (en) 2018-04-05
KR20190056432A (ko) 2019-05-24
ES2893532T3 (es) 2022-02-09
CL2019000902A1 (es) 2019-06-21
JP2019534876A (ja) 2019-12-05
ECSP19026680A (es) 2019-04-30
CN110036001A (zh) 2019-07-19
TN2020000158A1 (en) 2022-04-04
HUE056502T2 (hu) 2022-02-28
EP3523287A1 (en) 2019-08-14
US10703738B2 (en) 2020-07-07
JOP20190070B1 (ar) 2023-09-17
MA46452B1 (fr) 2021-10-29
CR20190168A (es) 2019-05-17
CY1124837T1 (el) 2022-11-25
TWI796306B (zh) 2023-03-21
HRP20211617T1 (hr) 2022-03-04
US10730849B2 (en) 2020-08-04
PH12019500712B1 (en) 2023-05-10
RS62410B1 (sr) 2021-10-29
MX2019003829A (es) 2019-07-01
PL3523287T3 (pl) 2021-12-20
IL265678B2 (en) 2023-06-01
PH12019500712A1 (en) 2019-12-02
CA3038903A1 (en) 2018-04-12
DK3523287T3 (da) 2021-10-18
CO2019003349A2 (es) 2019-04-12
DOP2019000083A (es) 2019-07-15
AR109788A1 (es) 2019-01-23
KR102312721B1 (ko) 2021-10-13
BR112019006816A8 (pt) 2023-02-07
SG10202008647TA (en) 2020-10-29
AU2017339418C1 (en) 2020-12-17
CN110036001B (zh) 2022-03-22
EA201990846A1 (ru) 2019-08-30
WO2018067423A1 (en) 2018-04-12
JP6636673B2 (ja) 2020-01-29
MA46452A (fr) 2021-04-07
AU2017339418B2 (en) 2020-04-16
SI3523287T1 (sl) 2021-11-30
US20190337918A1 (en) 2019-11-07
TN2020000159A1 (en) 2022-04-04
UA125223C2 (uk) 2022-02-02
NI201900029A (es) 2019-05-13
AU2017339418A1 (en) 2019-04-18
PT3523287T (pt) 2021-10-06
MY196383A (en) 2023-03-28
MX386187B (es) 2025-03-18
TW201817723A (zh) 2018-05-16
US20190337917A1 (en) 2019-11-07

Similar Documents

Publication Publication Date Title
PE20190705A1 (es) COMPUESTOS DE BENZO[b] TIOFENO COMO AGONISTAS DE STING
CL2019002167A1 (es) Compuesto de la fórmula (ic) o una sal farmacéuticamente aceptable del mismo, o una composición farmacéutica que comprende dicho compuesto o una sal farmacéuticamente aceptable del mismo, y al menos un portador farmacéuticamente aceptable, y su uso en el tratamiento de disautonomía familiar al mejorar el empalme de marn. (divisional solicitud 201701823.)
CO2018010748A2 (es) Agentes antivirales contra la hepatitis b
UY37007A (es) Compuestos derivados de purinas, estimuladores de genes de interferón
PE20211655A1 (es) Compuestos de 6-azabencimidazol sustituidos como inhibidores de hpk1
UY38483A (es) Heterociclos funcionalizados como agentes antivirales
CO2018002060A2 (es) Compuestos farmacéuticos
PE20181298A1 (es) Inhibidores de bromodominio bivalentes y usos de los mismos
EA201992601A1 (ru) Конденсированное имидазопиперидиновое соединение, являющееся ингибитором jak
PE20181491A1 (es) Nuevos derivados biciclicos, un proceso para su preparacion y composiciones farmaceuticas que los contienen
DOP2016000316A (es) Dinucleótidos cíclicos como moduladores de sting
AR083849A1 (es) Antagonistas de mdm2 de espiro-oxindol
PE20181045A1 (es) Compuestos utiles como inmunomoduladores
EA201992126A1 (ru) Ингибиторы jak, содержащие 4-членный гетероциклический амид
PE20160875A1 (es) Compuestos de biaril-amida como inhibidores de cinasa
AR111494A1 (es) Compuestos de anilinoquinazolina c₅ y su uso en el tratamiento del cáncer
AR101177A1 (es) Inhibidores de la syk
AR103222A1 (es) Procedimiento para la preparación de análogos de 4-fenil-5-alcoxicarbonil-2-tiazol-2-il-1,4-dihidropirimidina
PE20191461A1 (es) Compuestos amida para el tratamiento del vih
ATE517882T1 (de) Chinolinderivate
WO2016081203A3 (en) Phospholipid ether analogs as cancer-targeting drug vehicles
PE20180461A1 (es) Nuevos compuestos biciclicos como inhibidores de la atx
PE20220567A1 (es) Nuevos derivados piperidinilo, un proceso para su preparacion y composiciones farmaceuticas que los contienen
EA202090514A1 (ru) Противовирусное средство против гепатита в
PE20151892A1 (es) Compuestos tetraciclicos sustituidos con heterociclo y metodos de uso de los mismos para el tratamiento de enfermedades viricas