CA3058654A1 - Methods and compositions for treating retina-associated disease using ccr3-inhibitors - Google Patents

Methods and compositions for treating retina-associated disease using ccr3-inhibitors Download PDF

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Publication number
CA3058654A1
CA3058654A1 CA3058654A CA3058654A CA3058654A1 CA 3058654 A1 CA3058654 A1 CA 3058654A1 CA 3058654 A CA3058654 A CA 3058654A CA 3058654 A CA3058654 A CA 3058654A CA 3058654 A1 CA3058654 A1 CA 3058654A1
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Prior art keywords
alkyl
optionally substituted
group
cndot
formula
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CA3058654A
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English (en)
French (fr)
Inventor
Laura Coradini
Sam JACKSON
Karoly Nikolich
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Alkahest Inc
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Publication of CA3058654A1 publication Critical patent/CA3058654A1/en
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    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic 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
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445Non condensed piperidines, e.g. piperocaine
    • A61K31/4523Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/4545Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. pipamperone, anabasine
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/535Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/53751,4-Oxazines, e.g. morpholine
    • A61K31/53771,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/14Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
    • A61K9/141Intimate drug-carrier mixtures characterised by the carrier, e.g. ordered mixtures, adsorbates, solid solutions, eutectica, co-dried, co-solubilised, co-kneaded, co-milled, co-ground products, co-precipitates, co-evaporates, co-extrudates, co-melts; Drug nanoparticles with adsorbed surface modifiers
    • A61K9/143Intimate drug-carrier mixtures characterised by the carrier, e.g. ordered mixtures, adsorbates, solid solutions, eutectica, co-dried, co-solubilised, co-kneaded, co-milled, co-ground products, co-precipitates, co-evaporates, co-extrudates, co-melts; Drug nanoparticles with adsorbed surface modifiers with inorganic compounds
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/14Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
    • A61K9/141Intimate drug-carrier mixtures characterised by the carrier, e.g. ordered mixtures, adsorbates, solid solutions, eutectica, co-dried, co-solubilised, co-kneaded, co-milled, co-ground products, co-precipitates, co-evaporates, co-extrudates, co-melts; Drug nanoparticles with adsorbed surface modifiers
    • A61K9/145Intimate drug-carrier mixtures characterised by the carrier, e.g. ordered mixtures, adsorbates, solid solutions, eutectica, co-dried, co-solubilised, co-kneaded, co-milled, co-ground products, co-precipitates, co-evaporates, co-extrudates, co-melts; Drug nanoparticles with adsorbed surface modifiers with organic compounds
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/20Pills, tablets, discs, rods
    • A61K9/2004Excipients; Inactive ingredients
    • A61K9/2013Organic compounds, e.g. phospholipids, fats
    • A61K9/2018Sugars, or sugar alcohols, e.g. lactose, mannitol; Derivatives thereof, e.g. polysorbates
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/20Pills, tablets, discs, rods
    • A61K9/2004Excipients; Inactive ingredients
    • A61K9/2022Organic macromolecular compounds
    • A61K9/2027Organic macromolecular compounds obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyvinyl pyrrolidone, poly(meth)acrylates
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/20Pills, tablets, discs, rods
    • A61K9/2004Excipients; Inactive ingredients
    • A61K9/2022Organic macromolecular compounds
    • A61K9/205Polysaccharides, e.g. alginate, gums; Cyclodextrin
    • A61K9/2054Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/20Pills, tablets, discs, rods
    • A61K9/2004Excipients; Inactive ingredients
    • A61K9/2022Organic macromolecular compounds
    • A61K9/205Polysaccharides, e.g. alginate, gums; Cyclodextrin
    • A61K9/2059Starch, including chemically or physically modified derivatives; Amylose; Amylopectin; Dextrin
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/20Pills, tablets, discs, rods
    • A61K9/28Dragees; Coated pills or tablets, e.g. with film or compression coating
    • A61K9/2806Coating materials
    • A61K9/2813Inorganic compounds
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/20Pills, tablets, discs, rods
    • A61K9/28Dragees; Coated pills or tablets, e.g. with film or compression coating
    • A61K9/2806Coating materials
    • A61K9/282Organic compounds, e.g. fats
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/20Pills, tablets, discs, rods
    • A61K9/28Dragees; Coated pills or tablets, e.g. with film or compression coating
    • A61K9/2806Coating materials
    • A61K9/2833Organic macromolecular compounds
    • A61K9/284Organic macromolecular compounds obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyvinyl pyrrolidone
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/20Pills, tablets, discs, rods
    • A61K9/28Dragees; Coated pills or tablets, e.g. with film or compression coating
    • A61K9/2806Coating materials
    • A61K9/2833Organic macromolecular compounds
    • A61K9/2853Organic macromolecular compounds obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyethylene glycol, polyethylene oxide, poloxamers, poly(lactide-co-glycolide)
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/20Pills, tablets, discs, rods
    • A61K9/28Dragees; Coated pills or tablets, e.g. with film or compression coating
    • A61K9/2806Coating materials
    • A61K9/2833Organic macromolecular compounds
    • A61K9/286Polysaccharides, e.g. gums; Cyclodextrin
    • A61K9/2866Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00Drugs for disorders of the senses
    • A61P27/02Ophthalmic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K2300/00Mixtures or combinations of active ingredients, wherein at least one active ingredient is fully defined in groups A61K31/00 - A61K41/00
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07BGENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00Indexing scheme relating to specific properties of organic compounds
    • C07B2200/13Crystalline forms, e.g. polymorphs

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Epidemiology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Organic Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Inorganic Chemistry (AREA)
  • Ophthalmology & Optometry (AREA)
  • Communicable Diseases (AREA)
  • Oncology (AREA)
  • Biophysics (AREA)
  • Molecular Biology (AREA)
  • Immunology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Quinoline Compounds (AREA)
  • Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Pyridine Compounds (AREA)
  • Medicinal Preparation (AREA)
  • Medicines Containing Plant Substances (AREA)
CA3058654A 2017-04-05 2018-04-04 Methods and compositions for treating retina-associated disease using ccr3-inhibitors Pending CA3058654A1 (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201762482134P 2017-04-05 2017-04-05
US62/482,134 2017-04-05
PCT/US2018/026091 WO2018187473A1 (en) 2017-04-05 2018-04-04 Methods and compositions for treating retina-associated disease using ccr3-inhibitors

Publications (1)

Publication Number Publication Date
CA3058654A1 true CA3058654A1 (en) 2018-10-11

Family

ID=62067800

Family Applications (1)

Application Number Title Priority Date Filing Date
CA3058654A Pending CA3058654A1 (en) 2017-04-05 2018-04-04 Methods and compositions for treating retina-associated disease using ccr3-inhibitors

Country Status (20)

Country Link
US (2) US11590118B2 (https=)
EP (2) EP3606521B1 (https=)
JP (1) JP7179755B2 (https=)
KR (1) KR102658724B1 (https=)
CN (1) CN110650740A (https=)
AU (2) AU2018248425B2 (https=)
BR (1) BR112019020430A2 (https=)
CA (1) CA3058654A1 (https=)
CL (1) CL2019002839A1 (https=)
CO (1) CO2019012336A2 (https=)
EA (1) EA201992356A1 (https=)
ES (2) ES2950453T3 (https=)
IL (1) IL269743B (https=)
MX (1) MX394915B (https=)
MY (1) MY199462A (https=)
NZ (1) NZ757769A (https=)
SG (1) SG11201909207VA (https=)
TW (1) TW201841636A (https=)
UA (1) UA125658C2 (https=)
WO (1) WO2018187473A1 (https=)

Families Citing this family (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
SG11201909245PA (en) * 2017-04-05 2019-11-28 Alkahest Inc Methods and compositions for treating aging-associated impairments using ccr3-inhibitors
CN112789044A (zh) * 2018-09-26 2021-05-11 万能溶剂有限公司 使用ccr3-抑制剂治疗衰老相关损伤的方法及组合物
AU2021287906B2 (en) * 2020-06-11 2025-09-11 Alkahest Inc. Methods of improving retina-associated disease outcome using CCR3-inhibitors
CN112322719A (zh) * 2020-11-06 2021-02-05 温州医科大学 循环血外泌体miRNA作为视网膜静脉阻塞疾病诊断标志物中的应用

Family Cites Families (9)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
RU2002112800A (ru) 2002-05-16 2004-03-10 Евгений Ильич Зарайский (RU) Способ лечения диабетической ретинопатии
US8008092B2 (en) 2007-10-09 2011-08-30 University Of Kentucky Research Foundation CCR3 inhibition for ocular angiogenesis and macular degeneration
US8278302B2 (en) * 2009-04-08 2012-10-02 Boehringer Ingelheim International Gmbh Substituted piperidines as CCR3 antagonists
UA109290C2 (uk) 2010-10-07 2015-08-10 Спільні кристали і солі інгібіторів ccr3
RU2014126070A (ru) 2011-12-01 2016-01-27 Глэксо Груп Лимитед Способы лечения и предотвращения глазных заболеваний
AR090566A1 (es) 2012-04-02 2014-11-19 Boehringer Ingelheim Int Proceso para la produccion de inhibidores de crr
US20130261153A1 (en) * 2012-04-03 2013-10-03 Boehringer Ingelheim International Gmbh Use of ccr3-inhibitors
US10213421B2 (en) * 2012-04-04 2019-02-26 Alkahest, Inc. Pharmaceutical formulations comprising CCR3 antagonists
SG11201909245PA (en) 2017-04-05 2019-11-28 Alkahest Inc Methods and compositions for treating aging-associated impairments using ccr3-inhibitors

Also Published As

Publication number Publication date
US11951102B2 (en) 2024-04-09
EP4245295A3 (en) 2023-11-01
MY199462A (en) 2023-10-30
ES3046717T3 (en) 2025-12-02
IL269743A (en) 2019-11-28
TW201841636A (zh) 2018-12-01
JP2020513004A (ja) 2020-04-30
US20240024305A1 (en) 2024-01-25
EP3606521B1 (en) 2023-04-19
EP4245295A2 (en) 2023-09-20
NZ757769A (en) 2025-10-31
JP7179755B2 (ja) 2022-11-29
KR20190131121A (ko) 2019-11-25
KR102658724B1 (ko) 2024-04-18
MX394915B (es) 2025-03-24
BR112019020430A2 (pt) 2021-03-30
EA201992356A1 (ru) 2020-03-23
CO2019012336A2 (es) 2020-04-01
US20210106577A1 (en) 2021-04-15
CN110650740A (zh) 2020-01-03
MX2019012012A (es) 2019-12-11
UA125658C2 (uk) 2022-05-11
IL269743B (en) 2022-09-01
US11590118B2 (en) 2023-02-28
AU2024204133B2 (en) 2026-03-26
ES2950453T3 (es) 2023-10-10
EP3606521A1 (en) 2020-02-12
AU2024204133A1 (en) 2024-07-04
CL2019002839A1 (es) 2020-06-05
WO2018187473A1 (en) 2018-10-11
SG11201909207VA (en) 2019-11-28
AU2018248425A1 (en) 2019-10-31
EP4245295B1 (en) 2025-08-06
AU2018248425B2 (en) 2024-03-28

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