AR112414A1 - Agonistas del receptor tipo toll 7 (tlr7) que tienen una porción benzotriazol, conjugados de estos y métodos y usos de estos - Google Patents
Agonistas del receptor tipo toll 7 (tlr7) que tienen una porción benzotriazol, conjugados de estos y métodos y usos de estosInfo
- Publication number
- AR112414A1 AR112414A1 ARP180102337A AR112414A1 AR 112414 A1 AR112414 A1 AR 112414A1 AR P180102337 A ARP180102337 A AR P180102337A AR 112414 A1 AR112414 A1 AR 112414A1
- Authority
- AR
- Argentina
- Prior art keywords
- alkyl
- cycloalkyl
- tlr7
- toll
- conjugates
- Prior art date
Links
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
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- 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
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- 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
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- 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
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- 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
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- 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
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Immunology (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Engineering & Computer Science (AREA)
- Epidemiology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Virology (AREA)
- Molecular Biology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicinal Preparation (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
Abstract
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. Reivindicación 1: Un compuesto caracterizado porque tiene una estructura de acuerdo con la fórmula (1), en donde R¹ es (C₁₋₅ alquil)O, (C₁₋₂ alquil)O(CH₂)₂₋₃O, (C₁₋₅ alquil)C(=O)O, (C₁₋₅ alquil)NH, (C₁₋₂ alquil)O(CH₂)₂₋₃NH o (C₁₋₅ alquil)C(=O)NH; R² es, independientemente de cada caso, H, C₁₋₃ alquilo, halo, O(C₁₋₃ alquilo), CN o NO₂; R³ es H, Me o (CH₂)ˣR⁴, en donde el subíndice x es 2, 3 ó 4; y R⁴ es H, halo, OH, CN, NH₂, NH(C₁₋₅ alquilo), N(C₁₋₅ alquilo)₂, NH(C₃₋₆ cicloalquilo), NH(C₄₋₈ bicicloalquilo), NH(C₆₋₁₀ espirocicloalquilo), N(C₃₋₆ cicloalquilo)₂, NH(CH₂)₁₋₃(arilo), N((CH₂)₁₋₃(arilo))₂, una porción amina cíclica que tiene la estructura de la fórmula (2), una porción aromática o heteroaromática de 6 miembros o una porción heteroaromática de 5 miembros; en donde una porción alquilo, cicloalquilo, bicicloalquilo, espirocicloalquilo, amina cíclica, aromática o heteroaromática de 6 miembros o heteroaromática de 5 miembros se sustituye opcionalmente con uno o más sustituyentes seleccionados de OH, halo, CN, (C₁₋₃ alquilo), O(C₁₋₃ alquilo), C(=O)(Me), SO₂(C₁₋₃ alquilo), C(=O)(Et), NH₂, NH(Me), N(Me)₂, NH(Et), N(Et)₂ y N(C₁₋₃ alquilo)₂; y una porción cicloalquilo, bicicloalquilo, espiroalquilo o amina cíclica puede tener un grupo CH₂ reemplazado por O, S, NH, N(C₁₋₃ alquilo) o N(Boc).
Applications Claiming Priority (1)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US201762546095P | 2017-08-16 | 2017-08-16 |
Publications (1)
Publication Number | Publication Date |
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AR112414A1 true AR112414A1 (es) | 2019-10-23 |
Family
ID=63713994
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
ARP180102337 AR112414A1 (es) | 2017-08-16 | 2018-08-15 | Agonistas del receptor tipo toll 7 (tlr7) que tienen una porción benzotriazol, conjugados de estos y métodos y usos de estos |
Country Status (9)
Country | Link |
---|---|
US (3) | US10472361B2 (es) |
EP (1) | EP3668872B1 (es) |
JP (2) | JP7159295B2 (es) |
KR (1) | KR20200041912A (es) |
CN (1) | CN111032657B (es) |
AR (1) | AR112414A1 (es) |
ES (1) | ES2908984T3 (es) |
TW (1) | TW201920180A (es) |
WO (1) | WO2019036023A1 (es) |
Families Citing this family (23)
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WO2018009916A1 (en) | 2016-07-07 | 2018-01-11 | The Board Of Trustees Of The Leland Stanford Junior University | Antibody adjuvant conjugates |
US10472361B2 (en) * | 2017-08-16 | 2019-11-12 | Bristol-Myers Squibb Company | Toll-like receptor 7 (TLR7) agonists having a benzotriazole moiety, conjugates thereof, and methods and uses therefor |
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 |
KR20210098488A (ko) | 2018-11-30 | 2021-08-10 | 브리스톨-마이어스 스큅 컴퍼니 | 글루타민-함유 경쇄 c-말단 연장부를 포함하는 항체, 그의 접합체, 및 방법 및 용도 |
US20220031860A1 (en) | 2018-12-12 | 2022-02-03 | Bristol-Myers Squibb Company | Antibodies modified for transglutaminase conjugation, conjugates thereof, and methods and uses |
BR112021015577A8 (pt) | 2019-02-08 | 2021-10-05 | Research & Business Found Sungkyunkwan Univ | Complexo-colesterol agonista do receptor toll-like 7/8, composição de nanopartícula, composição adjuvante, composição de vacina, composição para regular uma função imunológica, composição farmacêutica e uso do complexo |
WO2020190725A1 (en) | 2019-03-15 | 2020-09-24 | Bolt Biotherapeutics, Inc. | Immunoconjugates targeting her2 |
JP2023512228A (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 |
CN115279765A (zh) | 2020-01-27 | 2022-11-01 | 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 |
WO2021154667A1 (en) | 2020-01-27 | 2021-08-05 | Bristol-Myers Squibb Company | C3-SUBSTITUTED 1H-PYRAZOLO[4,3-d]PYRIMIDINE COMPOUNDS AS TOLL-LIKE RECEPTOR 7 (TLR7) AGONISTS |
JP2023512207A (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 |
WO2021154662A1 (en) | 2020-01-27 | 2021-08-05 | Bristol-Myers Squibb Company | 1H-PYRAZOLO[4,3-d]PYRIMIDINE COMPOUNDS AS TOLL-LIKE RECEPTOR 7 (TLR7) AGONISTS |
WO2021154661A1 (en) | 2020-01-27 | 2021-08-05 | Bristol-Myers Squibb Company | 1H-PYRAZOLO[4,3-d]PYRIMIDINE COMPOUNDS AS TOLL-LIKE RECEPTOR 7 (TLR7) AGONISTS |
WO2021154665A1 (en) | 2020-01-27 | 2021-08-05 | Bristol-Myers Squibb Company | 1H-PYRAZOLO[4,3-d]PYRIMIDINE COMPOUNDS AS TOLL-LIKE RECEPTOR 7 (TLR7) AGONISTS |
JP2023512227A (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 |
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 |
US20230100429A1 (en) | 2020-03-02 | 2023-03-30 | Progeneer Inc. | Live-pathogen-mimetic nanoparticles based on pathogen cell wall skeleton, and production method thereof |
JP2023536945A (ja) | 2020-08-04 | 2023-08-30 | プロジェニア インコーポレイテッド | 動力学的に作用するアジュバントアンサンブル |
US20230277525A1 (en) | 2020-08-04 | 2023-09-07 | Progeneer Inc | Conjugate of functional drug and toll-like receptor 7 or 8 agonist of which active site is temporarily inactivated and use thereof |
JP2023536953A (ja) | 2020-08-04 | 2023-08-30 | プロジェニア インコーポレイテッド | 動力学的制御が可能なアジュバントを含むmRNAワクチン |
CN114315861A (zh) * | 2020-09-27 | 2022-04-12 | 上海维申医药有限公司 | 大环tlr7激动剂、其制备方法、药物组合物及其用途 |
EP4232094A1 (en) | 2020-10-21 | 2023-08-30 | Univerza V Ljubljani | Conjugated tlr7 and nod2 agonists |
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- 2018-08-15 TW TW107128398A patent/TW201920180A/zh unknown
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JP7159295B2 (ja) | 2022-10-24 |
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JP2020531472A (ja) | 2020-11-05 |
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EP3668872A1 (en) | 2020-06-24 |
JP7474820B2 (ja) | 2024-04-25 |
US10941145B2 (en) | 2021-03-09 |
WO2019036023A1 (en) | 2019-02-21 |
KR20200041912A (ko) | 2020-04-22 |
CN111032657A (zh) | 2020-04-17 |
US20200024279A1 (en) | 2020-01-23 |
US10696676B2 (en) | 2020-06-30 |
JP2023011643A (ja) | 2023-01-24 |
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