AR109629A1 - COMPOSITIONS FOR THE LOCAL ADMINISTRATION OF TOLL TYPE RECEIVER AGONISTS - Google Patents

COMPOSITIONS FOR THE LOCAL ADMINISTRATION OF TOLL TYPE RECEIVER AGONISTS

Info

Publication number
AR109629A1
AR109629A1 ARP170102467A ARP170102467A AR109629A1 AR 109629 A1 AR109629 A1 AR 109629A1 AR P170102467 A ARP170102467 A AR P170102467A AR P170102467 A ARP170102467 A AR P170102467A AR 109629 A1 AR109629 A1 AR 109629A1
Authority
AR
Argentina
Prior art keywords
group
alkyl
alkylene
alkenyl
aryl
Prior art date
Application number
ARP170102467A
Other languages
Spanish (es)
Inventor
Janardhanan Anand Subramony
Alexander Schwarz
Amir Fakhari
Original Assignee
Medimmune Llc
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 Medimmune Llc filed Critical Medimmune Llc
Publication of AR109629A1 publication Critical patent/AR109629A1/en

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Classifications

    • 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
    • A61K31/4745—Quinolines; Isoquinolines ortho- or peri-condensed with heterocyclic ring systems condensed with ring systems having nitrogen as a ring hetero atom, e.g. phenantrolines
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • 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
    • A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
    • A61K47/08—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing oxygen, e.g. ethers, acetals, ketones, quinones, aldehydes, peroxides
    • A61K47/10—Alcohols; Phenols; Salts thereof, e.g. glycerol; Polyethylene glycols [PEG]; Poloxamers; PEG/POE alkyl ethers
    • 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
    • A61K47/30—Macromolecular organic or inorganic compounds, e.g. inorganic polyphosphates
    • A61K47/34—Macromolecular compounds obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyesters, polyamino acids, polysiloxanes, polyphosphazines, copolymers of polyalkylene glycol or poloxamers
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/0012—Galenical forms characterised by the site of application
    • A61K9/0019—Injectable compositions; Intramuscular, intravenous, arterial, subcutaneous administration; Compositions to be administered through the skin in an invasive manner
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/0012—Galenical forms characterised by the site of application
    • A61K9/0019—Injectable compositions; Intramuscular, intravenous, arterial, subcutaneous administration; Compositions to be administered through the skin in an invasive manner
    • A61K9/0024—Solid, semi-solid or solidifying implants, which are implanted or injected in body tissue
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/06—Ointments; Bases therefor; Other semi-solid forms, e.g. creams, sticks, gels
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/08—Solutions
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • C—CHEMISTRY; METALLURGY
    • C08—ORGANIC MACROMOLECULAR COMPOUNDS; THEIR PREPARATION OR CHEMICAL WORKING-UP; COMPOSITIONS BASED THEREON
    • C08K—Use of inorganic or non-macromolecular organic substances as compounding ingredients
    • C08K5/00—Use of organic ingredients
    • C08K5/16—Nitrogen-containing compounds
    • C08K5/34—Heterocyclic compounds having nitrogen in the ring
    • C08K5/3442—Heterocyclic compounds having nitrogen in the ring having two nitrogen atoms in the ring
    • C08K5/3445—Five-membered rings

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Epidemiology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Dermatology (AREA)
  • Engineering & Computer Science (AREA)
  • Biomedical Technology (AREA)
  • Neurosurgery (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Organic Chemistry (AREA)
  • Oil, Petroleum & Natural Gas (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Inorganic Chemistry (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicinal Preparation (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)

Abstract

Composiciones que comprenden un polímero termosensible inverso, un modificador de la respuesta inmunitaria (IRM) y etanol. El polímero termosensible es poloxamer 407 o PLGA-PEG-PLGA. El IRM puede ser un agonista de receptor de tipo Toll (TLR), en particular, un agonista de TLR7, TLR8 o TLR7/8. Métodos. Usos. Reivindicación 1: Una composición que comprende: a) un 10% - 25% (p/v) de un polímero termosensible inverso; b) un modificador de la respuesta inmunitaria (IRM) de fórmula (1), en donde R¹ tiene la fórmula alquileno-L-R¹⁻¹, alquenileno-L-R¹⁻¹ o alquinileno-L-R¹⁻¹, en donde: los grupos alquileno, alquenileno y alquinileno están opcionalmente interrumpidos o terminados por uno o más grupos -O-; L es un enlace o un grupo enlazador funcional seleccionado entre el grupo que consiste en -NH-S(O)₂-, -NH-C(O)-, -NH-C(S)-, -NH-S(O)₂-NR³-, -NH-C(O)-NR³-, -NH-C(S)-NR³-, -NH-C(O)-O-, -O-, -S- y -S(O)₂-; y R¹⁻¹ es un grupo alifático lineal o ramificado que incluye opcionalmente uno o mas enlaces carbono-carbono insaturados; R se selecciona entre el grupo que consiste en hidrógeno, halógeno, hidroxi, alquilo, alquenilo, haloalquilo, alcoxi, alquiltio y -N(R³)₂; n es de 0 a 4; R² se selecciona entre el grupo que consiste en: hidrógeno; alquilo; alquenilo; arilo; heteroarilo; heterociclilo; alquilen-Y-alquilo; alquilen-Y-alquenilo; alquilen-Y-arilo; y alquilo o alquenilo sustituido con uno o más sustituyentes seleccionados entre el grupo que consiste en: -OH; halógeno; -N(R⁴)₂; -C(O)alquilo C₁₋₁₀; -C(O)-O-alquilo C₁₋₁₀; -N₃; arilo; heteroarilo; heterociclilo; -C(O)-arilo; y -C(O)-heteroarilo; Y es -O- o -S(O)₀₋₂-; cada R⁴ se selecciona independientemente entre el grupo que consiste en hidrógeno, alquilo C₁₋₁₀ y alquenilo C₂₋₁₀; y R³ se selecciona entre el grupo que consiste en hidrógeno y alquilo; con la condición de que cuando L es -NH-S(O₂)- y n es 0, R¹⁻¹ sea un grupo alifático lineal o ramificado que tiene al menos 16 átomos de carbono que incluye opcionalmente uno o más enlaces carbono-carbono insaturados; o una sal farmacéuticamente aceptable del mismo; y c) hasta un 20% (v/v) de etanol.Compositions comprising a reverse thermosensitive polymer, an immune response modifier (MRI) and ethanol. The thermosensitive polymer is poloxamer 407 or PLGA-PEG-PLGA. The MRI may be a Toll-like receptor agonist (TLR), in particular, an agonist of TLR7, TLR8 or TLR7 / 8. Methods Applications. Claim 1: A composition comprising: a) 10% -25% (w / v) of a reverse thermosensitive polymer; b) an immune response modifier (MRI) of formula (1), wherein R¹ has the formula alkylene-L-R¹⁻¹, alkenylene-L-R¹⁻¹ or alkynylene-L-R¹⁻¹, wherein: alkylene, alkenylene and alkynylene groups are optionally interrupted or terminated by one or more -O- groups; L is a functional linker or linker group selected from the group consisting of -NH-S (O) ₂-, -NH-C (O) -, -NH-C (S) -, -NH-S (O ) ₂-NR³-, -NH-C (O) -NR³-, -NH-C (S) -NR³-, -NH-C (O) -O-, -O-, -S- and -S ( O) ₂-; and R¹⁻¹ is a linear or branched aliphatic group that optionally includes one or more unsaturated carbon-carbon bonds; R is selected from the group consisting of hydrogen, halogen, hydroxy, alkyl, alkenyl, haloalkyl, alkoxy, alkylthio and -N (R³) ₂; n is from 0 to 4; R² is selected from the group consisting of: hydrogen; I rent; alkenyl; aryl; heteroaryl; heterocyclyl; alkylene-Y-alkyl; alkylene-Y-alkenyl; alkylene-Y-aryl; and alkyl or alkenyl substituted with one or more substituents selected from the group consisting of: -OH; halogen; -N (R⁴) ₂; -C (O) C₁₋₁₀ alkyl; -C (O) -O-C₁₋₁₀ alkyl; -N₃; aryl; heteroaryl; heterocyclyl; -C (O) -aryl; and -C (O) -heteroaryl; Y is -O- or -S (O) ₀₋₂-; each R⁴ is independently selected from the group consisting of hydrogen, C₁₋₁₀ alkyl and C₂₋₁₀ alkenyl; and R³ is selected from the group consisting of hydrogen and alkyl; with the proviso that when L is -NH-S (O₂) - and n is 0, R¹⁻¹ is a linear or branched aliphatic group having at least 16 carbon atoms that optionally includes one or more unsaturated carbon-carbon bonds; or a pharmaceutically acceptable salt thereof; and c) up to 20% (v / v) ethanol.

ARP170102467A 2016-09-08 2017-09-06 COMPOSITIONS FOR THE LOCAL ADMINISTRATION OF TOLL TYPE RECEIVER AGONISTS AR109629A1 (en)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US201662384922P 2016-09-08 2016-09-08

Publications (1)

Publication Number Publication Date
AR109629A1 true AR109629A1 (en) 2019-01-09

Family

ID=61561541

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP170102467A AR109629A1 (en) 2016-09-08 2017-09-06 COMPOSITIONS FOR THE LOCAL ADMINISTRATION OF TOLL TYPE RECEIVER AGONISTS

Country Status (3)

Country Link
AR (1) AR109629A1 (en)
TW (1) TW201822767A (en)
WO (1) WO2018049017A1 (en)

Families Citing this family (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
KR20210141461A (en) 2019-02-01 2021-11-23 캔웰 바이오테크 리미티드 Imidazoquinoline amine derivatives, pharmaceutical compositions, uses thereof
CN113730570A (en) * 2019-09-26 2021-12-03 苏州百迈生物医药有限公司 Chemotherapy immune combined medicine and application thereof
WO2022093658A1 (en) * 2020-11-01 2022-05-05 Tianxin Wang In situ vaccine for cancer cell and tumor treatment

Family Cites Families (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20040265351A1 (en) * 2003-04-10 2004-12-30 Miller Richard L. Methods and compositions for enhancing immune response
CA2578741C (en) * 2004-09-02 2014-01-14 3M Innovative Properties Company 1-alkoxy 1h-imidazo ring systems and methods
US20100028381A1 (en) * 2006-06-19 2010-02-04 3M Innovative Properties Company Formulation for delivery of immune response modifiers
US20160000890A1 (en) * 2013-03-15 2016-01-07 Biospecifics Technologies Corp. Thermosensitive hydrogel collagenase formulations
US10682415B2 (en) * 2013-07-22 2020-06-16 Wisconsin Alumni Research Foundation Thermogel formulation for combination drug delivery
US9980956B2 (en) * 2014-08-01 2018-05-29 3M Innovative Properties Company Methods and therapeutic combinations for treating tumors

Also Published As

Publication number Publication date
TW201822767A (en) 2018-07-01
WO2018049017A1 (en) 2018-03-15

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