HRP20201043T1 - Spojevi 4-amino-imidazokinolina - Google Patents
Spojevi 4-amino-imidazokinolina Download PDFInfo
- Publication number
- HRP20201043T1 HRP20201043T1 HRP20201043TT HRP20201043T HRP20201043T1 HR P20201043 T1 HRP20201043 T1 HR P20201043T1 HR P20201043T T HRP20201043T T HR P20201043TT HR P20201043 T HRP20201043 T HR P20201043T HR P20201043 T1 HRP20201043 T1 HR P20201043T1
- Authority
- HR
- Croatia
- Prior art keywords
- formula
- compound
- quinolin
- imidazo
- ethoxymethyl
- Prior art date
Links
- RSYUXZQXNGSKGO-UHFFFAOYSA-N 1h-imidazo[4,5-h]quinolin-4-amine Chemical class NC1=CC2=CC=CN=C2C2=C1N=CN2 RSYUXZQXNGSKGO-UHFFFAOYSA-N 0.000 title 1
- 150000001875 compounds Chemical class 0.000 claims 22
- 150000003839 salts Chemical class 0.000 claims 6
- 229910052739 hydrogen Inorganic materials 0.000 claims 5
- 239000001257 hydrogen Substances 0.000 claims 5
- 125000006239 protecting group Chemical group 0.000 claims 4
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 claims 2
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 2
- CBIHUSLWRFJGHZ-UHFFFAOYSA-N NC1=NC=2C=C(C=CC2C2=C1N=C(N2CC(C)(C)OCCN)COCC)CCC(=O)OCC Chemical compound NC1=NC=2C=C(C=CC2C2=C1N=C(N2CC(C)(C)OCCN)COCC)CCC(=O)OCC CBIHUSLWRFJGHZ-UHFFFAOYSA-N 0.000 claims 2
- AMFXKVJFWIICMM-UHFFFAOYSA-N NCC(=O)OC(CN1C(=NC=2C(=NC=3C=CC=CC3C21)N)COCC)(C)C Chemical compound NCC(=O)OC(CN1C(=NC=2C(=NC=3C=CC=CC3C21)N)COCC)(C)C AMFXKVJFWIICMM-UHFFFAOYSA-N 0.000 claims 2
- MMGIMCFVDIHCIY-UHFFFAOYSA-N NCCOC(CN1C(=NC=2C(=NC=3C=CC=CC3C21)N)COCC)(C)C Chemical compound NCCOC(CN1C(=NC=2C(=NC=3C=CC=CC3C21)N)COCC)(C)C MMGIMCFVDIHCIY-UHFFFAOYSA-N 0.000 claims 2
- 239000002253 acid Substances 0.000 claims 2
- 238000006243 chemical reaction Methods 0.000 claims 2
- 230000008878 coupling Effects 0.000 claims 2
- 238000010168 coupling process Methods 0.000 claims 2
- 238000005859 coupling reaction Methods 0.000 claims 2
- 239000003814 drug Substances 0.000 claims 2
- 125000002485 formyl group Chemical class [H]C(*)=O 0.000 claims 2
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims 2
- 238000000034 method Methods 0.000 claims 2
- 125000006701 (C1-C7) alkyl group Chemical group 0.000 claims 1
- NIXOWILDQLNWCW-UHFFFAOYSA-M Acrylate Chemical compound [O-]C(=O)C=C NIXOWILDQLNWCW-UHFFFAOYSA-M 0.000 claims 1
- 208000023275 Autoimmune disease Diseases 0.000 claims 1
- 208000035143 Bacterial infection Diseases 0.000 claims 1
- 208000035473 Communicable disease Diseases 0.000 claims 1
- 208000031888 Mycoses Diseases 0.000 claims 1
- SCCSYTVGXWOGDH-UHFFFAOYSA-N NC1=NC=2C=C(C=CC2C2=C1N=C(N2CC(C)(C)OC(CN)=O)COCC)CCC(=O)OCC Chemical compound NC1=NC=2C=C(C=CC2C2=C1N=C(N2CC(C)(C)OC(CN)=O)COCC)CCC(=O)OCC SCCSYTVGXWOGDH-UHFFFAOYSA-N 0.000 claims 1
- RNJCSLXTDAQCMP-UHFFFAOYSA-N NCCOC(CN1C(=NC=2C(=NC=3C=C(C=CC3C21)Br)N)COCC)(C)C Chemical compound NCCOC(CN1C(=NC=2C(=NC=3C=C(C=CC3C21)Br)N)COCC)(C)C RNJCSLXTDAQCMP-UHFFFAOYSA-N 0.000 claims 1
- UKWYNGPGDNDJRN-UHFFFAOYSA-N NCCOC(CN1C(=NC=2C(=NC=3C=CC=CC3C21)N)CCCCC)(C)C Chemical compound NCCOC(CN1C(=NC=2C(=NC=3C=CC=CC3C21)N)CCCCC)(C)C UKWYNGPGDNDJRN-UHFFFAOYSA-N 0.000 claims 1
- 206010028980 Neoplasm Diseases 0.000 claims 1
- 208000030852 Parasitic disease Diseases 0.000 claims 1
- 230000002378 acidificating effect Effects 0.000 claims 1
- 201000011510 cancer Diseases 0.000 claims 1
- 150000001732 carboxylic acid derivatives Chemical class 0.000 claims 1
- 239000003638 chemical reducing agent Substances 0.000 claims 1
- 238000010511 deprotection reaction Methods 0.000 claims 1
- 201000010099 disease Diseases 0.000 claims 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 239000012374 esterification agent Substances 0.000 claims 1
- 125000005448 ethoxyethyl group Chemical group [H]C([H])([H])C([H])([H])OC([H])([H])C([H])([H])* 0.000 claims 1
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims 1
- 229910052736 halogen Inorganic materials 0.000 claims 1
- 150000002367 halogens Chemical group 0.000 claims 1
- 150000002431 hydrogen Chemical group 0.000 claims 1
- 238000004519 manufacturing process Methods 0.000 claims 1
- 239000000825 pharmaceutical preparation Substances 0.000 claims 1
- 239000000126 substance Substances 0.000 claims 1
- 230000003612 virological effect Effects 0.000 claims 1
Classifications
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- C—CHEMISTRY; METALLURGY
- 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
- A61K31/4164—1,3-Diazoles
- A61K31/4188—1,3-Diazoles condensed with other heterocyclic ring systems, e.g. biotin, sorbinil
-
- 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
- A61K31/435—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
-
- 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
- A61K31/435—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
- A61K31/47—Quinolines; Isoquinolines
- A61K31/4738—Quinolines; Isoquinolines ortho- or peri-condensed with heterocyclic ring systems
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/12—Antivirals
- A61P31/20—Antivirals for DNA viruses
-
- 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
-
- 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
- A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
-
- 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
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- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Immunology (AREA)
- Engineering & Computer Science (AREA)
- Epidemiology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Oncology (AREA)
- Communicable Diseases (AREA)
- Virology (AREA)
- Biotechnology (AREA)
- Molecular Biology (AREA)
- Transplantation (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)
Claims (11)
1. Spoj, naznačen time, da ima formulu
[image]
u kojoj
R1 je C1−7-alkil ili C1−7-alkoksi-C1−7-alkil;
R2 je odabran iz skupine koju čine vodik, halogen, C1-7-alkoksikarbonil-C1−7-alkil i C1-7-alkoksikarbonil-C2−7-alkenil;
R3 je vodik;
R4 je odabran iz skupine koja se sastoji od -O-(CH2)m-NHR5, i -O-(CO)-(CH2)n-NHR6,
pri čemu
m je 2,
n je 1,
R5 je vodik i
R6 je vodik;
ili njihovih farmaceutski prihvatljivih soli.
2. Spoj koji ima formulu I prema patentnom zahtjevu 1, naznačen time, da R1 je C1−7-alkoksi-C1−7-alkil.
3. Spoj koji ima formulu I prema patentnim zahtjevima 1 ili 2, naznačen time, da R1 je etoksietil.
4. Spoj koji ima formulu I prema bilo kojem od patentnih zahtjeva 1 do 3, naznačen time, da R2 je vodik.
5. Spoj koji ima formulu I prema patentnom zahtjevu 1, naznačen time, da je odabran iz skupine koja se sastoji od:
1-(2-(2-aminoetoksi)-2-metilpropil)-2-(etoksimetil)-1H-imidazo[4,5-c]kinolin-4-amina,
1-(4-amino-2-(etoksimetil)-1H-imidazo[4,5-c]kinolin-1-il)-2-metilpropan-2-il-2-aminoacetata,
etil (E)-3-[4-amino-1-[2-(2-aminoetoksi)-2-metilpropil]-2-(etoksimetil)-1H-imidazo[4,5-c]kinolin-7-il]prop-2-enoata,
etil 3-(4-amino-1-(2-(2-aminoetoksi)-2-metilpropil)-2-(etoksimetil)-1H-imidazo[4,5-c]kinolin-7-il)propanoata,
etil 3-(4-amino-1-(2-(2-aminoacetoksi)-2-metilpropil)-2-(etoksimetil)-1H- imidazo[4,5-c]kinolin-7-il)propanoata,
1-(2-(2-aminoetoksi)-2-metilpropil)-2-pentil-1H-imidazo[4,5-c]kinolin-4-amina,
1-(2-(2-aminoetoksi)-2-metilpropil)-7-bromo-2-(etoksimetil)-1H-imidazo[4,5-c]kinolin-4-amina,
i njihovih farmaceutski prihvatljivih soli.
6. Spoj koji ima formulu I prema patentnom zahtjevu 1, naznačen time, da je to:
1-(2-(2-aminoetoksi)-2-metilpropil)-2-(etoksimetil)-1H-imidazo[4,5-c]kinolin-4-amin,
i njegove farmaceutski prihvatljive soli.
7. Spoj koji ima formulu I prema patentnom zahtjevu 1, naznačen time, da je odabran iz skupine koja se sastoji od:
1-(4-amino-2-(etoksimetil)-1H-imidazo[4,5-c]kinolin-1-il)-2-metilpropan-2-il-2-aminoacetata,
etil 3-(4-amino-1-(2-(2-aminoetoksi)-2-metilpropil)-2-(etoksimetil)-1H-imidazo[4,5-c]kinolin-7-il)propanoata,
i njegovih farmaceutski prihvatljivih soli.
8. Spoj koji ima formulu I prema bilo kojem od patentnih zahtjeva 1 do 7, naznačen time, da se koristi kao lijek.
9. Spoj koji ima formulu I prema bilo kojem od patentnih zahtjeva 1 do 7, naznačen time, da se koristi kao lijek za liječenje raka ili autoimunih bolesti ili zaraznih bolesti odabranih iz skupine koja se sastoji od virusnih bolesti, bakterijskih bolesti, gljivičnih bolesti i parazitskih bolesti.
10. Farmaceutski pripravak, naznačen time, da sadrži spoj sa formulom I prema bilo kojem od patentnih zahtjeva 1 do 7 i farmaceutski prihvatljiv nosač i/ili pomoćnu tvar.
11. Postupak proizvodnje spoja sa formulom I definiranom prema patentnom zahtjevu 1, naznačen time, da postupak obuhvaća:
a) reakciju spoja koji ima formulu II
[image]
i time, da su R1, R2 i R3 definirani prema patentnom zahtjevu 1, te time, da je PG zaštitna grupa, sa spojem koji ima formulu III
[image]
pri čemu je m definirano prema patentnom zahtjevu 1, pod osnovnim uvjetima, i uklanjanje zaštitnih grupa PG i Boc u kiselim uvjetima, kako bi se dobio spoj koji ima formulu I-a
[image]
gdje su R1 do R3 i m definirani prema patentnom zahtjevu 1, i po izboru daljnje spajanje spoja koji ima formulu I-a s alkoholom ili kiselinom formule R5-OH ili aldehidom formule R5=O, kako bi se dobio spoj koji ima formulu I-c
[image]
pri čemu su R1 do R3, m i R5 definirani prema patentnom zahtjevu 1, te po izboru, pretvaranje dobivenog spoja u farmaceutski prihvatljivu sol, ili
b) reakciju spoja koji ima formulu II-a
[image]
u kojoj su R1, R2 i R3 definirani prema patentnom zahtjevu 1 i time, da je PG’ zaštitna grupa, s karboksilnom kiselinom koja ima formulu IV
[image]
gdje je n definirano prema patentnom zahtjevu 1 i PG" je zaštitna grupa, u prisustvu agensa za esterifikaciju te uklanjanje zaštitnih grupa PG' i PG" s blagim reducirajućim agensom, kako bi se dobio spoj koji ima formulu I-b
[image]
u kojoj su R1 do R3 i n definirani prema patentnom zahtjevu 1, i po izboru, daljnje spajanje spoja formule I-a s alkoholom ili kiselinom formule R6-OH ili aldehidom formule R6=O, kako bi se dobio spoj koji ima formulu I-d
[image]
gdje su R1 do R3, m i R6 definirani prema patentnom zahtjevu 1, i po izboru, pretvaranje dobivenog spoja u farmaceutski prihvatljivu sol.
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP14165349 | 2014-04-22 | ||
| PCT/EP2015/058465 WO2015162075A1 (en) | 2014-04-22 | 2015-04-20 | 4-amino-imidazoquinoline compounds |
| EP15716824.6A EP3134402B1 (en) | 2014-04-22 | 2015-04-20 | 4-amino-imidazoquinoline compounds |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| HRP20201043T1 true HRP20201043T1 (hr) | 2020-10-16 |
Family
ID=50489008
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| HRP20201043TT HRP20201043T1 (hr) | 2014-04-22 | 2020-07-01 | Spojevi 4-amino-imidazokinolina |
Country Status (22)
| Country | Link |
|---|---|
| US (2) | US9334268B2 (hr) |
| EP (1) | EP3134402B1 (hr) |
| JP (1) | JP6367366B2 (hr) |
| KR (1) | KR101905292B1 (hr) |
| CN (1) | CN106232599B (hr) |
| AR (1) | AR100137A1 (hr) |
| BR (1) | BR112016017261B1 (hr) |
| CA (1) | CA2938280C (hr) |
| DK (1) | DK3134402T3 (hr) |
| ES (1) | ES2804101T3 (hr) |
| HR (1) | HRP20201043T1 (hr) |
| HU (1) | HUE049656T2 (hr) |
| LT (1) | LT3134402T (hr) |
| MA (1) | MA39898B1 (hr) |
| MX (1) | MX2016013689A (hr) |
| PL (1) | PL3134402T3 (hr) |
| PT (1) | PT3134402T (hr) |
| RS (1) | RS60430B1 (hr) |
| RU (1) | RU2698902C2 (hr) |
| SI (1) | SI3134402T1 (hr) |
| TW (1) | TWI607007B (hr) |
| WO (1) | WO2015162075A1 (hr) |
Families Citing this family (71)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2017102652A1 (en) * | 2015-12-14 | 2017-06-22 | Glaxosmithkline Biologicals S.A. | Pegylated imidazoquinolines as tlr7 and tlr8 agonists |
| PT3889145T (pt) | 2015-12-17 | 2024-04-02 | Merck Patent Gmbh | 8-ciano-5-piperidino-quinolinas como antagonistas de tlr7/8 e suas utilizações para tratamento de distúrbios imunitários |
| EP3464274B1 (en) | 2016-05-23 | 2020-05-27 | H. Hoffnabb-La Roche Ag | Benzazepine dicarboxamide compounds with secondary amide function |
| JP6918838B2 (ja) | 2016-05-23 | 2021-08-11 | エフ・ホフマン−ラ・ロシュ・アクチェンゲゼルシャフト | 第三級アミド基を有するベンズアゼピンジカルボキサミド化合物 |
| WO2017216054A1 (en) | 2016-06-12 | 2017-12-21 | F. Hoffmann-La Roche Ag | Dihydropyrimidinyl benzazepine carboxamide compounds |
| BR112019000071A2 (pt) | 2016-07-07 | 2019-07-02 | Bolt Biotherapeutics Inc | conjugados adjuvantes de anticorpo |
| RU2758686C2 (ru) | 2016-08-08 | 2021-11-01 | Мерк Патент Гмбх | Антагонисты tlr7/8 и их применение |
| DK3526323T3 (da) | 2016-10-14 | 2023-06-26 | Prec Biosciences Inc | Modificerede meganucleaser der er specifikke for en genkendelsessekvens i hepatitis b virusgenomet |
| CA3044903A1 (en) * | 2016-11-28 | 2018-05-31 | Jiangsu Hengrui Medicine Co., Ltd. | Pyrazolo-heteroaryl derivative, preparation method and medical use thereof |
| US10757485B2 (en) * | 2017-08-25 | 2020-08-25 | Honda Motor Co., Ltd. | System and method for synchronized vehicle sensor data acquisition processing using vehicular communication |
| WO2019084060A1 (en) | 2017-10-24 | 2019-05-02 | Silverback Therapeutics, Inc. | CONJUGATES AND METHODS OF USE FOR THE SELECTIVE DELIVERY OF IMMUNOMODULATORY AGENTS |
| WO2019118884A1 (en) | 2017-12-15 | 2019-06-20 | Silverback Therapeutics, Inc. | Antibody construct-drug conjugate for the treatment of hepatitis |
| 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 |
| CA3084569A1 (en) | 2017-12-20 | 2019-06-27 | Institute Of Organic Chemistry And Biochemistry Ascr, V.V.I. | 3'3' cyclic dinucleotides with phosphonate bond activating the sting adaptor protein |
| EP3728255B1 (en) | 2017-12-20 | 2022-01-26 | 3M Innovative Properties Company | Amide substituted imidazo[4,5-c]quinoline compounds with a branched chain linking group for use as an immune response modifier |
| CN108299421B (zh) * | 2018-01-30 | 2020-09-29 | 中国医学科学院药用植物研究所 | 一种瑞喹莫德的酰化衍生物及制备方法与应用 |
| CA3091142C (en) | 2018-02-26 | 2023-04-11 | Gilead Sciences, Inc. | Substituted pyrrolizine compounds and uses thereof |
| US11370788B2 (en) | 2018-02-28 | 2022-06-28 | 3M Innovative Properties Company | Substituted imidazo[4,5-c]quinoline compounds with an N-1 branched group |
| 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 |
| TW201945388A (zh) | 2018-04-12 | 2019-12-01 | 美商精密生物科學公司 | 對b型肝炎病毒基因體中之識別序列具有特異性之最佳化之經工程化巨核酸酶 |
| TW202014193A (zh) | 2018-05-03 | 2020-04-16 | 捷克科學院有機化學與生物化學研究所 | 包含碳環核苷酸之2’3’－環二核苷酸 |
| EP3802536B1 (en) | 2018-05-24 | 2022-07-13 | 3M Innovative Properties Company | N-1 branched cycloalkyl substituted imidazo[4,5-c]quinoline compounds, compositions, and methods |
| CN110526917B (zh) * | 2018-05-25 | 2021-09-03 | 江苏恒瑞医药股份有限公司 | 一种吡唑并杂芳基类衍生物的可药用盐、晶型及其制备方法 |
| CN111819178B (zh) * | 2018-05-25 | 2022-04-12 | 江苏恒瑞医药股份有限公司 | 一种吡唑并杂芳基类衍生物盐酸盐的晶型及制备方法 |
| CN110526918B (zh) * | 2018-05-25 | 2021-09-03 | 江苏恒瑞医药股份有限公司 | 一种吡唑并杂芳基类衍生物的晶型及制备方法 |
| 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 |
| CN112888677A (zh) | 2018-08-16 | 2021-06-01 | 先天肿瘤免疫公司 | 被取代的4-氨基-1H-咪唑并[4,5-c]喹啉化合物及其改进的制备方法 |
| WO2020051356A1 (en) * | 2018-09-07 | 2020-03-12 | Birdie Biopharmaceuticals, Inc. | Imidazoquinoline compounds and uses thereof |
| WO2020056192A1 (en) * | 2018-09-12 | 2020-03-19 | Silverback Therapeutics, Inc. | Antibody conjugates of toll-like receptor agonists |
| BR112021004590A2 (pt) | 2018-09-12 | 2021-05-25 | Silverback Therapeutics, Inc. | composições para o tratamento de doença com conjugados imunoestimuladores |
| TW202136260A (zh) | 2018-10-31 | 2021-10-01 | 美商基利科學股份有限公司 | 經取代之6-氮雜苯并咪唑化合物 |
| TW202136261A (zh) | 2018-10-31 | 2021-10-01 | 美商基利科學股份有限公司 | 經取代之6-氮雜苯并咪唑化合物 |
| AU2020216345A1 (en) * | 2019-02-01 | 2021-08-26 | Canwell Biotech Limited | Imidazoquinoline amine derivatives, pharmaceutical composition, use thereof |
| AU2020231201A1 (en) | 2019-03-07 | 2021-08-26 | Institute Of Organic Chemistry And Biochemistry Ascr, V.V.I. | 2'3'-cyclic dinucleotides and prodrugs thereof |
| US20220143061A1 (en) | 2019-03-07 | 2022-05-12 | Institute Of Organic Chemistry And Biochemistry Ascr, V.V.I. | 3'3'-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 |
| KR20220004634A (ko) | 2019-03-15 | 2022-01-11 | 볼트 바이오테라퓨틱스 인코퍼레이티드 | Her2를 표적으로 하는 면역접합체 |
| TW202210480A (zh) | 2019-04-17 | 2022-03-16 | 美商基利科學股份有限公司 | 類鐸受體調節劑之固體形式 |
| TW202212339A (zh) | 2019-04-17 | 2022-04-01 | 美商基利科學股份有限公司 | 類鐸受體調節劑之固體形式 |
| US11453681B2 (en) | 2019-05-23 | 2022-09-27 | Gilead Sciences, Inc. | Substituted eneoxindoles and uses thereof |
| US20220249685A1 (en) | 2019-06-19 | 2022-08-11 | Silverback Therapeutics, Inc. | Anti-mesothelin antibodies and immunoconjugates thereof |
| CN112174903B (zh) * | 2019-07-01 | 2022-07-12 | 清华大学 | Tlr8的小分子调节剂 |
| US11339159B2 (en) | 2019-07-17 | 2022-05-24 | Pfizer Inc. | Toll-like receptor agonists |
| US20220296619A1 (en) | 2019-08-19 | 2022-09-22 | Gilead Sciences, Inc. | Pharmaceutical formulations of tenofovir alafenamide |
| US11497808B2 (en) | 2019-09-30 | 2022-11-15 | Gilead Sciences, Inc. | HBV vaccines and methods treating HBV |
| AU2020358726A1 (en) | 2019-10-01 | 2022-04-07 | Silverback Therapeutics, Inc. | Combination therapy with immune stimulatory conjugates |
| CN114599360A (zh) * | 2019-10-29 | 2022-06-07 | 骏达贸易有限公司 | 4-氨基-咪唑并喹啉化合物及其用途 |
| WO2021113765A1 (en) | 2019-12-06 | 2021-06-10 | Precision Biosciences, Inc. | Optimized engineered meganucleases having specificity for a recognition sequence in the hepatitis b virus genome |
| EP4106819A1 (en) | 2020-02-21 | 2022-12-28 | Silverback Therapeutics, Inc. | Nectin-4 antibody conjugates and uses thereof |
| CN115605493A (zh) | 2020-03-20 | 2023-01-13 | 吉利德科学公司（Us） | 4′-c-取代的-2-卤代-2′-脱氧腺苷核苷的前药及其制备和使用方法 |
| US20230338395A1 (en) | 2020-04-19 | 2023-10-26 | Ludwig Englmeier | Prophylaxis and treatment of coronavirus infection |
| IL298124A (en) * | 2020-05-14 | 2023-01-01 | Merck Healthcare Kgaa | Tlr7/8 antagonists for the treatment of corona virus infection |
| EP4153590A4 (en) * | 2020-05-21 | 2024-06-19 | Ohio State Innovation Foundation | FUNCTIONAL LIPID DERIVATIVES AND THEIR USES |
| EP4175673A1 (en) | 2020-07-01 | 2023-05-10 | ARS Pharmaceuticals Inc. | Anti-asgr1 antibody conjugates and uses thereof |
| WO2022153157A1 (en) * | 2021-01-13 | 2022-07-21 | Pfizer Inc. | A crystalline form of 2-((4-amino-2-(ethoxymethyl)-6,7-dimethyl-1 h-imidazo[4,5-c]pyridin-1-yl)methyl)-2-methylpropane-1,3-diol free base |
| AR124812A1 (es) * | 2021-02-03 | 2023-05-10 | Seagen Inc | Conjugados y compuestos inmunoestimulantes |
| CN117279664A (zh) | 2021-04-10 | 2023-12-22 | 普方生物制药美国公司 | Folr1结合剂、其偶联物及其使用方法 |
| JP2024516631A (ja) | 2021-04-23 | 2024-04-16 | プロファウンドバイオ ユーエス カンパニー | 抗ｃｄ７０抗体、そのコンジュゲートおよびこれを使用する方法 |
| US20240269142A1 (en) | 2021-05-13 | 2024-08-15 | Gilead Sciences, Inc. | COMBINATION OF A TLR8 MODULATING COMPOUND AND ANTI-HBV siRNA THERAPEUTICS |
| JP2024520593A (ja) | 2021-06-23 | 2024-05-24 | ギリアード サイエンシーズ， インコーポレイテッド | ジアシルグリエルコール（ｄｉａｃｙｌｇｌｙｅｒｃｏｌ）キナーゼ調節化合物 |
| WO2022271684A1 (en) | 2021-06-23 | 2022-12-29 | Gilead Sciences, Inc. | Diacylglyercol kinase modulating compounds |
| 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 |
| EP4359413A1 (en) | 2021-06-23 | 2024-05-01 | Gilead Sciences, Inc. | Diacylglyercol kinase modulating compounds |
| TW202320857A (zh) | 2021-07-06 | 2023-06-01 | 美商普方生物製藥美國公司 | 連接子、藥物連接子及其結合物及其使用方法 |
| WO2023081237A1 (en) * | 2021-11-03 | 2023-05-11 | Regents Of The University Of Minnesota | Toll-like receptor agonists and antagonists and uses thereof |
| WO2024030577A1 (en) * | 2022-08-03 | 2024-02-08 | Seagen Inc. | Immunostimulatory anti-pd-l1-drug conjugates |
| WO2024100093A1 (en) * | 2022-11-09 | 2024-05-16 | Merck Patent Gmbh | Toll-like receptor 7 agonists as immune-stimulators to elicit the innate antitumor immunity |
| WO2024112932A1 (en) * | 2022-11-23 | 2024-05-30 | Regents Of The University Of Minnesota | Immunomodulators and immunomodulator conjugates |
Family Cites Families (21)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| SG70625A1 (en) * | 1991-03-01 | 2000-02-22 | Minnesota Mining & Mfg | 1-Substituted 2-substituted 1H-imidazo(4, 5-c) quinolin-4-amines |
| US6451810B1 (en) * | 1999-06-10 | 2002-09-17 | 3M Innovative Properties Company | Amide substituted imidazoquinolines |
| US6664265B2 (en) * | 2000-12-08 | 2003-12-16 | 3M Innovative Properties Company | Amido ether substituted imidazoquinolines |
| US6861440B2 (en) * | 2001-10-26 | 2005-03-01 | Hoffmann-La Roche Inc. | DPP IV inhibitors |
| DK1719511T3 (da) * | 2001-11-16 | 2009-04-14 | Coley Pharm Group Inc | N-[4-(4-amino-2-ethyl-1H-imidazo[4,5-c]quinolin-1-yl)butyl]methansulfonamid, en farmaceutisk sammensætning omfattende samme, og anvendelse deraf |
| GEP20084545B (en) * | 2003-09-05 | 2008-11-25 | Anadys Pharmaceuticals Inc | Introducing tlr7 ligands and prodrugs thereof for the treatment of hepatitis c viral infection |
| AU2004315771A1 (en) * | 2003-12-04 | 2005-08-25 | 3M Innovative Properties Company | Sulfone substituted imidazo ring ethers |
| TW201402124A (zh) | 2005-08-19 | 2014-01-16 | Array Biopharma Inc | 作為類鐸受體（ｔｏｌｌ-ｌｉｋｅ ｒｅｃｅｐｔｏｒ）調節劑之８-經取代苯并氮雜呯 |
| CA2716706C (en) | 2008-03-03 | 2014-02-18 | Irm Llc | Compounds and compositions as tlr activity modulators |
| EP2358683B1 (en) | 2008-11-06 | 2015-04-01 | VentiRx Pharmaceuticals, Inc. | Methods of synthesis of benzazepine derivatives |
| EP2396328A2 (en) | 2009-02-11 | 2011-12-21 | The Regents of The University of California | Toll-like receptor modulators and treatment of diseases |
| TR201909600T4 (tr) | 2009-08-07 | 2019-07-22 | Glaxosmithkline Biologicals Sa | Lipide edilmiş oksoadenin türevleri. |
| WO2011068233A1 (en) | 2009-12-03 | 2011-06-09 | Dainippon Sumitomo Pharma Co., Ltd. | Imidazoquinolines which act via toll - like receptors (tlr) |
| CN103118682A (zh) | 2010-04-30 | 2013-05-22 | 加利福尼亚大学校务委员会 | 合成tlr7激动剂的磷脂缀合物的用途 |
| NZ608673A (en) | 2010-10-01 | 2015-04-24 | Univ Pennsylvania | Therapeutic use of a tlr agonist and combination therapy |
| WO2012066336A1 (en) | 2010-11-19 | 2012-05-24 | Astrazeneca Ab | Benzylamine compounds as toll -like receptor 7 agonists |
| US9107958B2 (en) | 2011-06-03 | 2015-08-18 | 3M Innovative Properties Company | Hydrazino 1H-imidazoquinolin-4-amines and conjugates made therefrom |
| WO2012167801A1 (ru) | 2011-06-07 | 2012-12-13 | Uglovsky Sergey Evgenievich | Импульсная установка для преобразования низкопотенциальной тепловой энергии в электрическую |
| US9034336B2 (en) | 2011-08-30 | 2015-05-19 | Regents Of The University Of Minnesota | Immunomodulators and immunomodulator conjugates |
| CN104661683A (zh) * | 2011-11-09 | 2015-05-27 | 埃森德生物制药有限公司 | 免疫调节缀合物 |
| WO2013166110A1 (en) | 2012-05-02 | 2013-11-07 | Yale University | Tlr-agonist-conjugated antibody recruiting molecules (tlr_arms) |
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| EP3134402A1 (en) | 2017-03-01 |
| EP3134402B1 (en) | 2020-05-06 |
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| JP2017513883A (ja) | 2017-06-01 |
| US20150299194A1 (en) | 2015-10-22 |
| CA2938280C (en) | 2022-07-12 |
| KR20160138317A (ko) | 2016-12-02 |
| KR101905292B1 (ko) | 2018-11-21 |
| ES2804101T3 (es) | 2021-02-03 |
| CA2938280A1 (en) | 2015-10-29 |
| CN106232599B (zh) | 2018-11-16 |
| RS60430B1 (sr) | 2020-07-31 |
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| US20160222010A1 (en) | 2016-08-04 |
| BR112016017261A8 (pt) | 2020-06-16 |
| LT3134402T (lt) | 2020-07-10 |
| WO2015162075A1 (en) | 2015-10-29 |
| DK3134402T3 (da) | 2020-07-20 |
| RU2698902C2 (ru) | 2019-09-02 |
| BR112016017261B1 (pt) | 2022-04-19 |
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| US9447097B2 (en) | 2016-09-20 |
| MX2016013689A (es) | 2017-01-20 |
| HUE049656T2 (hu) | 2020-10-28 |
| TWI607007B (zh) | 2017-12-01 |
| AR100137A1 (es) | 2016-09-14 |
| JP6367366B2 (ja) | 2018-08-01 |
| MA39898B1 (fr) | 2020-08-31 |
| RU2016144386A3 (hr) | 2018-11-27 |
| RU2016144386A (ru) | 2018-05-22 |
| PL3134402T3 (pl) | 2020-11-02 |
| TW201544505A (zh) | 2015-12-01 |
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