MX2020001734A - Derivados de 6-amino-7,9-dihidro-8h-purina-8-ona como agonistas inmunoestimulantes del receptor 7 tipo toll (tlr7). - Google Patents
Derivados de 6-amino-7,9-dihidro-8h-purina-8-ona como agonistas inmunoestimulantes del receptor 7 tipo toll (tlr7).Info
- Publication number
- MX2020001734A MX2020001734A MX2020001734A MX2020001734A MX2020001734A MX 2020001734 A MX2020001734 A MX 2020001734A MX 2020001734 A MX2020001734 A MX 2020001734A MX 2020001734 A MX2020001734 A MX 2020001734A MX 2020001734 A MX2020001734 A MX 2020001734A
- Authority
- MX
- Mexico
- Prior art keywords
- sup
- tlr7
- toll
- agonists
- receptor
- Prior art date
Links
- 102000008236 Toll-Like Receptor 7 Human genes 0.000 title abstract 3
- 108010060825 Toll-Like Receptor 7 Proteins 0.000 title abstract 3
- 239000000556 agonist Substances 0.000 title abstract 2
- RGKBRPAAQSHTED-UHFFFAOYSA-N 8-oxoadenine Chemical class NC1=NC=NC2=C1NC(=O)N2 RGKBRPAAQSHTED-UHFFFAOYSA-N 0.000 title 1
- 229960001438 immunostimulant agent Drugs 0.000 title 1
- 239000003022 immunostimulating agent Substances 0.000 title 1
- 230000003308 immunostimulating effect Effects 0.000 title 1
- 150000001875 compounds Chemical class 0.000 abstract 2
- 239000002671 adjuvant Substances 0.000 abstract 1
- 210000000987 immune system Anatomy 0.000 abstract 1
- 210000000056 organ Anatomy 0.000 abstract 1
- 230000004936 stimulating effect Effects 0.000 abstract 1
Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D473/00—Heterocyclic compounds containing purine ring systems
- C07D473/02—Heterocyclic compounds containing purine ring systems with oxygen, sulphur, or nitrogen atoms directly attached in positions 2 and 6
- C07D473/18—Heterocyclic compounds containing purine ring systems with oxygen, sulphur, or nitrogen atoms directly attached in positions 2 and 6 one oxygen and one nitrogen atom, e.g. guanine
-
- 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
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
- A61K31/52—Purines, e.g. adenine
- A61K31/522—Purines, e.g. adenine having oxo groups directly attached to the heterocyclic ring, e.g. hypoxanthine, guanine, acyclovir
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
- A61K47/50—Medicinal 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
- A61K47/51—Medicinal 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
- A61K47/56—Medicinal 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 organic macromolecular compound, e.g. an oligomeric, polymeric or dendrimeric molecule
- A61K47/59—Medicinal 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 organic macromolecular compound, e.g. an oligomeric, polymeric or dendrimeric molecule obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyureas or polyurethanes
- A61K47/60—Medicinal 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 organic macromolecular compound, e.g. an oligomeric, polymeric or dendrimeric molecule obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyureas or polyurethanes the organic macromolecular compound being a polyoxyalkylene oligomer, polymer or dendrimer, e.g. PEG, PPG, PEO or polyglycerol
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
- A61K47/50—Medicinal 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
- A61K47/51—Medicinal 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
- A61K47/68—Medicinal 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
- A61K47/6889—Conjugates wherein the antibody being the modifying agent and wherein the linker, binder or spacer confers particular properties to the conjugates, e.g. peptidic enzyme-labile linkers or acid-labile linkers, providing for an acid-labile immuno conjugate wherein the drug may be released from its antibody conjugated part in an acidic, e.g. tumoural or environment
-
- 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
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
- A61K47/50—Medicinal 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
- A61K47/51—Medicinal 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
- A61K47/68—Medicinal 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
- A61K47/6835—Medicinal 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 the modifying agent being an antibody or an immunoglobulin bearing at least one antigen-binding site
- A61K47/6839—Medicinal 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 the modifying agent being an antibody or an immunoglobulin bearing at least one antigen-binding site the antibody targeting material from viruses
- A61K47/6841—Medicinal 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 the modifying agent being an antibody or an immunoglobulin bearing at least one antigen-binding site the antibody targeting material from viruses the antibody targeting a RNA virus
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Immunology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Epidemiology (AREA)
- Virology (AREA)
- Molecular Biology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicinal Preparation (AREA)
- Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)
- Peptides Or Proteins (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
Abstract
Compuestos que tienen una estructura de acuerdo con la Fórmula (I) o (II) (ver Fórmulas) en donde R1, R2, R3, R4, Ar y X1 son como se definen en la presente, son agonistas del receptor tipo toll 7 (TLR7) y se pueden usar como adyuvantes para estimular el sistema inmunitario. Algunos de estos compuestos se pueden usar en conjugados para la administración dirigida a un órgano o tejido de la acción prevista.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201762546222P | 2017-08-16 | 2017-08-16 | |
| PCT/US2018/000246 WO2019035971A1 (en) | 2017-08-16 | 2018-08-16 | 6-AMINO-7,9-DIHYDRO-8H-PURIN-8-ONE DERIVATIVES AS TOLL 7 RECEPTOR IMMUNOSTIMULATING AGONISTS (TLR7) |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| MX2020001734A true MX2020001734A (es) | 2020-03-20 |
Family
ID=63528885
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| MX2020001734A MX2020001734A (es) | 2017-08-16 | 2018-08-16 | Derivados de 6-amino-7,9-dihidro-8h-purina-8-ona como agonistas inmunoestimulantes del receptor 7 tipo toll (tlr7). |
Country Status (18)
| Country | Link |
|---|---|
| US (4) | US10508115B2 (es) |
| EP (1) | EP3668871B1 (es) |
| JP (1) | JP7228570B2 (es) |
| KR (1) | KR20200041910A (es) |
| CN (1) | CN111201228B (es) |
| AR (1) | AR112689A1 (es) |
| AU (1) | AU2018317860A1 (es) |
| BR (1) | BR112020003108A2 (es) |
| CA (1) | CA3073013A1 (es) |
| CO (1) | CO2020001498A2 (es) |
| EA (1) | EA202090495A1 (es) |
| ES (1) | ES2887253T3 (es) |
| IL (1) | IL272626A (es) |
| MX (1) | MX2020001734A (es) |
| PE (1) | PE20200835A1 (es) |
| SG (1) | SG11202001255WA (es) |
| TW (1) | TW201920181A (es) |
| WO (1) | WO2019035971A1 (es) |
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| AU2017292934B9 (en) | 2016-07-07 | 2024-08-29 | Bolt Biotherapeutics, Inc. | Antibody adjuvant conjugates |
| WO2019209811A1 (en) | 2018-04-24 | 2019-10-31 | Bristol-Myers Squibb Company | Macrocyclic toll-like receptor 7 (tlr7) agonists |
| US11554120B2 (en) | 2018-08-03 | 2023-01-17 | Bristol-Myers Squibb Company | 1H-pyrazolo[4,3-d]pyrimidine compounds as toll-like receptor 7 (TLR7) agonists and methods and uses therefor |
| SG11202101980VA (en) | 2018-09-12 | 2021-03-30 | Silverback Therapeutics Inc | Methods and composition for the treatment of disease with immune stimulatory conjugates |
| ES2943474T3 (es) | 2018-11-30 | 2023-06-13 | Bristol Myers Squibb Co | Anticuerpo que comprende una extensión carboxiterminal de una cadena ligera que contiene glutamina, conjugados del mismo, y métodos y usos |
| CN113544155A (zh) | 2018-12-12 | 2021-10-22 | 百时美施贵宝公司 | 经修饰用于转谷氨酰胺酶缀合的抗体、其缀合物以及方法和用途 |
| JP7287708B2 (ja) | 2019-02-08 | 2023-06-06 | プロジェニア インコーポレイテッド | Toll-like受容体7または8アゴニストとコレステロールの結合体およびその用途 |
| AU2020241686A1 (en) | 2019-03-15 | 2021-11-04 | Bolt Biotherapeutics, Inc. | Immunoconjugates targeting HER2 |
| KR102732033B1 (ko) * | 2019-07-26 | 2024-11-20 | 아주대학교산학협력단 | Tlr7 및 tlr9의 신호전달 경로를 억제하는 신규한 소분자 화합물 및 그 용도 |
| TW202126658A (zh) * | 2019-09-29 | 2021-07-16 | 大陸商江蘇恆瑞醫藥股份有限公司 | 吡咯并雜芳基衍生物或其偶聯物、其製備方法及其應用 |
| CA3151322A1 (en) | 2019-10-01 | 2021-04-08 | Silverback Therapeutics, Inc. | Combination therapy with immune stimulatory conjugates |
| US20230348468A1 (en) * | 2020-01-27 | 2023-11-02 | Bristol-Myers Squibb Company | 1H-PYRAZOLO[4,3-d]PYRIMIDINE COMPOUNDS AS TOLL-LIKE RECEPTOR 7 (TLR7) AGONISTS |
| KR20220132595A (ko) | 2020-01-27 | 2022-09-30 | 브리스톨-마이어스 스큅 컴퍼니 | 톨-유사 수용체 7 (TLR7) 효능제로서의 C3-치환된 1H-피라졸로[4,3-d]피리미딘 화합물 |
| EP4097105A1 (en) | 2020-01-27 | 2022-12-07 | Bristol-Myers Squibb Company | 1h-pyrazolo[4,3-d]pyrimidine compounds as toll-like receptor 7 (tlr7) agonists |
| EP4097101A1 (en) | 2020-01-27 | 2022-12-07 | Bristol-Myers Squibb Company | 1h-pyrazolo[4,3-d]pyrimidine compounds as toll-like receptor 7 (tlr7) agonists |
| EP4097103A1 (en) | 2020-01-27 | 2022-12-07 | Bristol-Myers Squibb Company | 1h-pyrazolo[4,3-d]pyrimidine compounds as toll-like receptor 7 (tlr7) agonists |
| KR20220132591A (ko) | 2020-01-27 | 2022-09-30 | 브리스톨-마이어스 스큅 컴퍼니 | 톨-유사 수용체 7 (TLR7) 효능제로서의 1H-피라졸로[4,3-d]피리미딘 화합물 |
| CN115210236A (zh) | 2020-01-27 | 2022-10-18 | 百时美施贵宝公司 | 作为Toll样受体7(TLR7)激动剂的1H-吡唑并[4,3-d]嘧啶化合物 |
| JP2023512208A (ja) | 2020-01-27 | 2023-03-24 | ブリストル-マイヤーズ スクイブ カンパニー | トール様受容体7(TLR7)アゴニストとしての1H-ピラゾロ[4,3-d]ピリミジン化合物 |
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| CN113797354B (zh) * | 2020-06-11 | 2024-08-13 | 江苏恒瑞医药股份有限公司 | 吡咯并嘧啶衍生物或其偶联物、其制备方法及其应用 |
| KR20230047361A (ko) | 2020-07-01 | 2023-04-07 | 아르스 파마슈티컬스 인크. | 항-asgr1 항체 접합체 및 이의 용도 |
| WO2022031021A1 (ko) | 2020-08-04 | 2022-02-10 | 성균관대학교산학협력단 | 동력학적 제어가 가능한 아주번트를 포함하는 mrna 백신 |
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| JP2023536954A (ja) | 2020-08-04 | 2023-08-30 | プロジェニア インコーポレイテッド | 活性化部位が一時的に不活性化したトール様受容体7または8作用薬と機能性薬物の結合体およびその用途 |
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-
2018
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- 2018-08-15 AR ARP180102341 patent/AR112689A1/es unknown
- 2018-08-15 TW TW107128399A patent/TW201920181A/zh unknown
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- 2018-08-16 KR KR1020207007180A patent/KR20200041910A/ko not_active Ceased
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| TW201920181A (zh) | 2019-06-01 |
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| EP3668871A1 (en) | 2020-06-24 |
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| US10689382B2 (en) | 2020-06-23 |
| PE20200835A1 (es) | 2020-08-13 |
| EA202090495A1 (ru) | 2020-05-28 |
| EP3668871B1 (en) | 2021-08-04 |
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