[go: up one dir, main page]

PE20170024A1 - Compuestos de 6,8-dioxabiciclo [3.2.1] octano-2,3-diol sustituidos como agentes de direccionamiento al asgpr - Google Patents

Compuestos de 6,8-dioxabiciclo [3.2.1] octano-2,3-diol sustituidos como agentes de direccionamiento al asgpr

Info

Publication number
PE20170024A1
PE20170024A1 PE2016002255A PE2016002255A PE20170024A1 PE 20170024 A1 PE20170024 A1 PE 20170024A1 PE 2016002255 A PE2016002255 A PE 2016002255A PE 2016002255 A PE2016002255 A PE 2016002255A PE 20170024 A1 PE20170024 A1 PE 20170024A1
Authority
PE
Peru
Prior art keywords
compounds
dioxabicyclo
asgpr
octane
tetraoxatridecan
Prior art date
Application number
PE2016002255A
Other languages
English (en)
Inventor
Spiros Liras
Benjamin Thuma
Vincent Mascitti
Original Assignee
Pfizer
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 Pfizer filed Critical Pfizer
Publication of PE20170024A1 publication Critical patent/PE20170024A1/es

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07H—SUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
    • C07H13/00—Compounds containing saccharide radicals esterified by carbonic acid or derivatives thereof, or by organic acids, e.g. phosphonic acids
    • C07H13/02—Compounds containing saccharide radicals esterified by carbonic acid or derivatives thereof, or by organic acids, e.g. phosphonic acids by carboxylic acids
    • C07H13/04—Compounds containing saccharide radicals esterified by carbonic acid or derivatives thereof, or by organic acids, e.g. phosphonic acids by carboxylic acids having the esterifying carboxyl radicals attached to acyclic carbon atoms
    • 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
    • A61K31/70—Carbohydrates; Sugars; Derivatives thereof
    • A61K31/7042—Compounds having saccharide radicals and heterocyclic rings
    • A61K31/7052—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides
    • A61K31/706—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom
    • 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
    • A61K31/70—Carbohydrates; Sugars; Derivatives thereof
    • A61K31/7008—Compounds having an amino group directly attached to a carbon atom of the saccharide radical, e.g. D-galactosamine, ranimustine
    • 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
    • A61K31/70—Carbohydrates; Sugars; Derivatives thereof
    • A61K31/7042—Compounds having saccharide radicals and heterocyclic rings
    • A61K31/7052—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides
    • A61K31/7056—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing five-membered rings with nitrogen as a ring hetero atom
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00—Medicinal preparations containing peptides
    • A61K38/16—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
    • A61K38/43—Enzymes; Proenzymes; Derivatives thereof
    • A61K38/46—Hydrolases (3)
    • A61K38/465—Hydrolases (3) acting on ester bonds (3.1), e.g. lipases, ribonucleases
    • 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
    • A61K47/54—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 compound
    • A61K47/545—Heterocyclic compounds
    • 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
    • A61K47/54—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 compound
    • A61K47/549—Sugars, nucleosides, nucleotides or nucleic acids
    • 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
    • A61K47/62—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 a protein, peptide or polyamino acid
    • A61K47/64—Drug-peptide, drug-protein or drug-polyamino acid conjugates, i.e. the modifying agent being a peptide, protein or polyamino acid which is covalently bonded or complexed to a therapeutically active agent
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/06—Antihyperlipidemics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • 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
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A61P7/04—Antihaemorrhagics; Procoagulants; Haemostatic agents; Antifibrinolytic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D309/00—Heterocyclic compounds containing six-membered rings having one oxygen atom as the only ring hetero atom, not condensed with other rings
    • C07D309/02—Heterocyclic compounds containing six-membered rings having one oxygen atom as the only ring hetero atom, not condensed with other rings having no double bonds between ring members or between ring members and non-ring members
    • C07D309/08—Heterocyclic compounds containing six-membered rings having one oxygen atom as the only ring hetero atom, not condensed with other rings having no double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D309/14—Nitrogen atoms not forming part of a nitro radical
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/14—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D493/00—Heterocyclic compounds containing oxygen atoms as the only ring hetero atoms in the condensed system
    • C07D493/02—Heterocyclic compounds containing oxygen atoms as the only ring hetero atoms in the condensed system in which the condensed system contains two hetero rings
    • C07D493/08—Bridged systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07H—SUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
    • C07H13/00—Compounds containing saccharide radicals esterified by carbonic acid or derivatives thereof, or by organic acids, e.g. phosphonic acids
    • C07H13/02—Compounds containing saccharide radicals esterified by carbonic acid or derivatives thereof, or by organic acids, e.g. phosphonic acids by carboxylic acids
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07H—SUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
    • C07H13/00—Compounds containing saccharide radicals esterified by carbonic acid or derivatives thereof, or by organic acids, e.g. phosphonic acids
    • C07H13/12—Compounds containing saccharide radicals esterified by carbonic acid or derivatives thereof, or by organic acids, e.g. phosphonic acids by acids having the group -X-C(=X)-X-, or halides thereof, in which each X means nitrogen, oxygen, sulfur, selenium or tellurium, e.g. carbonic acid, carbamic acid
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07H—SUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
    • C07H15/00—Compounds containing hydrocarbon or substituted hydrocarbon radicals directly attached to hetero atoms of saccharide radicals
    • C07H15/02—Acyclic radicals, not substituted by cyclic structures
    • C07H15/04—Acyclic radicals, not substituted by cyclic structures attached to an oxygen atom of the saccharide radical
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07H—SUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
    • C07H15/00—Compounds containing hydrocarbon or substituted hydrocarbon radicals directly attached to hetero atoms of saccharide radicals
    • C07H15/02—Acyclic radicals, not substituted by cyclic structures
    • C07H15/04—Acyclic radicals, not substituted by cyclic structures attached to an oxygen atom of the saccharide radical
    • C07H15/08—Polyoxyalkylene derivatives
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07H—SUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
    • C07H15/00—Compounds containing hydrocarbon or substituted hydrocarbon radicals directly attached to hetero atoms of saccharide radicals
    • C07H15/02—Acyclic radicals, not substituted by cyclic structures
    • C07H15/12—Acyclic radicals, not substituted by cyclic structures attached to a nitrogen atom of the saccharide radical
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07H—SUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
    • C07H15/00—Compounds containing hydrocarbon or substituted hydrocarbon radicals directly attached to hetero atoms of saccharide radicals
    • C07H15/26—Acyclic or carbocyclic radicals, substituted by hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07H—SUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
    • C07H9/00—Compounds containing a hetero ring sharing at least two hetero atoms with a saccharide radical
    • C07H9/02—Compounds containing a hetero ring sharing at least two hetero atoms with a saccharide radical the hetero ring containing only oxygen as ring hetero atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/06—Dipeptides
    • C07K5/06008—Dipeptides with the first amino acid being neutral
    • C07K5/06078—Dipeptides with the first amino acid being neutral and aromatic or cycloaliphatic
    • C—CHEMISTRY; METALLURGY
    • C12—BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
    • C12N—MICROORGANISMS OR ENZYMES; COMPOSITIONS THEREOF; PROPAGATING, PRESERVING, OR MAINTAINING MICROORGANISMS; MUTATION OR GENETIC ENGINEERING; CULTURE MEDIA
    • C12N9/00—Enzymes; Proenzymes; Compositions thereof; Processes for preparing, activating, inhibiting, separating or purifying enzymes
    • C12N9/14—Hydrolases (3)
    • C12N9/16—Hydrolases (3) acting on ester bonds (3.1)
    • C12N9/22—Ribonucleases [RNase]; Deoxyribonucleases [DNase]
    • C—CHEMISTRY; METALLURGY
    • C12—BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
    • C12Y—ENZYMES
    • C12Y301/00—Hydrolases acting on ester bonds (3.1)
    • Y—GENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
    • Y02—TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
    • Y02A—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE
    • Y02A50/00—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE in human health protection, e.g. against extreme weather
    • Y02A50/30—Against vector-borne diseases, e.g. mosquito-borne, fly-borne, tick-borne or waterborne diseases whose impact is exacerbated by climate change

Landscapes

  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Molecular Biology (AREA)
  • Engineering & Computer Science (AREA)
  • Medicinal Chemistry (AREA)
  • Genetics & Genomics (AREA)
  • Biochemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Biotechnology (AREA)
  • Epidemiology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Crystallography & Structural Chemistry (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Diabetes (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Hematology (AREA)
  • Immunology (AREA)
  • Obesity (AREA)
  • Biophysics (AREA)
  • Wood Science & Technology (AREA)
  • Zoology (AREA)
  • Biomedical Technology (AREA)
  • Microbiology (AREA)
  • General Engineering & Computer Science (AREA)
  • Emergency Medicine (AREA)
  • Endocrinology (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Peptides Or Proteins (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)

Abstract

Se refiere a compuestos de formula A, en donde: R1 es CN, CH2-CN, C=CH, CH2-N3, CH2-NH2, entre otros; y R2 es OH, N3, N(R3)2, N(R3)-C(O)-R3, entre otros. Estos compuestos se emplean como agentes de direccionamiento a un receptor de asialoglicoproteina (ASGPR) y se usan en el tratamiento de enfermedades hepaticas o condiciones moduladas por el higado incluyendo angioedema hereditario, tirosinemia familiar de tipo I, sindrome de Alagille, sintesis de acido biliar, hepatitis neonatal, entre otros. Entre los compuestos preferidos tenemos los siguientes: (4-((2-((1-(1-((1S,2R,3R,4R,5S)-4-acetamido-2,3-dihidroxi-6,8-dioxabiciclo[3,2,1]octan-1-il)-2,5,8,11-tetraoxatridecan-13-il)-1H-1,2,3-triazol-4-il)metoxi)etil)amino-4-oxobutil)carbamato de bencilo; (4-((1,3-bis-((1-(1-((1S,2R,3R,4R,5S)-4-acetamido-2,3-dihidroxi-6,8-dioxabiciclo[3,2,1]octan-1-il)-2,5,8,11-tetraoxatridecan-13-il)-1H-1,2,3-triazol-4-il)metoxi)propan-2-il)amino-4-oxobutil)carbamato de bencilo; entre otros.
PE2016002255A 2014-05-19 2015-05-05 Compuestos de 6,8-dioxabiciclo [3.2.1] octano-2,3-diol sustituidos como agentes de direccionamiento al asgpr PE20170024A1 (es)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201462000211P 2014-05-19 2014-05-19
US201462001540P 2014-05-21 2014-05-21
US201562139254P 2015-03-27 2015-03-27

Publications (1)

Publication Number Publication Date
PE20170024A1 true PE20170024A1 (es) 2017-03-17

Family

ID=53200246

Family Applications (1)

Application Number Title Priority Date Filing Date
PE2016002255A PE20170024A1 (es) 2014-05-19 2015-05-05 Compuestos de 6,8-dioxabiciclo [3.2.1] octano-2,3-diol sustituidos como agentes de direccionamiento al asgpr

Country Status (26)

Country Link
US (5) US9340553B2 (es)
EP (1) EP3145934B1 (es)
JP (2) JP6193513B2 (es)
KR (1) KR102149572B1 (es)
CN (1) CN106459120A (es)
AU (1) AU2015262993B2 (es)
BR (1) BR112016026809A2 (es)
CA (1) CA2891717C (es)
DK (1) DK3145934T5 (es)
ES (1) ES2841400T3 (es)
HU (1) HUE052146T2 (es)
IL (1) IL248667B (es)
MX (1) MX381383B (es)
MY (1) MY181586A (es)
NZ (1) NZ725600A (es)
PE (1) PE20170024A1 (es)
PH (1) PH12016502304A1 (es)
PL (1) PL3145934T3 (es)
PT (1) PT3145934T (es)
RU (1) RU2696490C2 (es)
SA (1) SA516380328B1 (es)
SG (1) SG11201608936UA (es)
SI (1) SI3145934T1 (es)
TW (1) TWI579286B (es)
UY (1) UY36126A (es)
WO (1) WO2015177668A1 (es)

Families Citing this family (53)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US11998479B2 (en) 2011-02-04 2024-06-04 Seed Health, Inc. Method and system for addressing adverse effects on the oral microbiome and restoring gingival health caused by sodium lauryl sulphate exposure
US12257272B2 (en) 2015-12-24 2025-03-25 Seed Health, Inc. Method and system for reducing the likelihood of developing depression in an individual
US11273187B2 (en) 2015-11-30 2022-03-15 Joseph E. Kovarik Method and system for reducing the likelihood of developing depression in an individual
US11523934B2 (en) 2011-02-04 2022-12-13 Seed Health, Inc. Method and system to facilitate the growth of desired bacteria in a human's mouth
US12279989B2 (en) 2011-02-04 2025-04-22 Seed Health, Inc. Method and system for increasing beneficial bacteria and decreasing pathogenic bacteria in the oral cavity
US10512661B2 (en) 2011-02-04 2019-12-24 Joseph E. Kovarik Method and system for reducing the likelihood of developing liver cancer in an individual diagnosed with non-alcoholic fatty liver disease
US9987224B2 (en) 2011-02-04 2018-06-05 Joseph E. Kovarik Method and system for preventing migraine headaches, cluster headaches and dizziness
US11951139B2 (en) 2015-11-30 2024-04-09 Seed Health, Inc. Method and system for reducing the likelihood of osteoporosis
US11419903B2 (en) 2015-11-30 2022-08-23 Seed Health, Inc. Method and system for reducing the likelihood of osteoporosis
US10548761B2 (en) 2011-02-04 2020-02-04 Joseph E. Kovarik Method and system for reducing the likelihood of colorectal cancer in a human being
US10842834B2 (en) 2016-01-06 2020-11-24 Joseph E. Kovarik Method and system for reducing the likelihood of developing liver cancer in an individual diagnosed with non-alcoholic fatty liver disease
US11951140B2 (en) 2011-02-04 2024-04-09 Seed Health, Inc. Modulation of an individual's gut microbiome to address osteoporosis and bone disease
US10687975B2 (en) 2011-02-04 2020-06-23 Joseph E. Kovarik Method and system to facilitate the growth of desired bacteria in a human's mouth
US12533312B2 (en) 2011-02-04 2026-01-27 Seed Health, Inc. Method and system for preventing sore throat in humans
US11844720B2 (en) 2011-02-04 2023-12-19 Seed Health, Inc. Method and system to reduce the likelihood of dental caries and halitosis
US10245288B2 (en) 2011-02-04 2019-04-02 Joseph E. Kovarik Method and system for reducing the likelihood of developing NASH in an individual diagnosed with non-alcoholic fatty liver disease
US10086018B2 (en) 2011-02-04 2018-10-02 Joseph E. Kovarik Method and system for reducing the likelihood of colorectal cancer in a human being
US12005085B2 (en) 2013-12-20 2024-06-11 Seed Health, Inc. Probiotic method and composition for maintaining a healthy vaginal microbiome
US11839632B2 (en) 2013-12-20 2023-12-12 Seed Health, Inc. Topical application of CRISPR-modified bacteria to treat acne vulgaris
US12329783B2 (en) 2013-12-20 2025-06-17 Seed Health, Inc. Method and system to improve the health of a person's skin microbiome
US12246043B2 (en) 2013-12-20 2025-03-11 Seed Health, Inc. Topical application to treat acne vulgaris
US11826388B2 (en) 2013-12-20 2023-11-28 Seed Health, Inc. Topical application of Lactobacillus crispatus to ameliorate barrier damage and inflammation
US11833177B2 (en) 2013-12-20 2023-12-05 Seed Health, Inc. Probiotic to enhance an individual's skin microbiome
US11998574B2 (en) 2013-12-20 2024-06-04 Seed Health, Inc. Method and system for modulating an individual's skin microbiome
US11969445B2 (en) 2013-12-20 2024-04-30 Seed Health, Inc. Probiotic composition and method for controlling excess weight, obesity, NAFLD and NASH
US11980643B2 (en) 2013-12-20 2024-05-14 Seed Health, Inc. Method and system to modify an individual's gut-brain axis to provide neurocognitive protection
DK3145934T5 (da) 2014-05-19 2020-11-30 Pfizer Substituerede-6,8-dioxabicyclo[3.2.1]octan-2,3-diol-forbindelser som ASGPR-targeteringsmidler
JP2018537448A (ja) * 2015-11-12 2018-12-20 ファイザー・インコーポレイテッド ＣＲＩＳＰＲ−Ｃａｓ９を用いた組織特異的ゲノム操作
US12239706B2 (en) 2015-11-30 2025-03-04 Seed Health, Inc. Method and system for protecting monarch butterflies from pesticides
US20230097887A1 (en) 2018-04-09 2023-03-30 Yale University Bi-functional Molecules to Degrade Circulating Proteins
CN112236169A (zh) 2018-04-09 2021-01-15 耶鲁大学 靶向循环蛋白质的选择性降解的双功能小分子
WO2019199621A1 (en) * 2018-04-09 2019-10-17 Yale University Bi-functional molecules to degrade circulating proteins
US12485178B2 (en) 2018-04-09 2025-12-02 Yale University Bifunctional small molecules to target the selective degradation of circulating proteins
US12150967B2 (en) 2018-08-18 2024-11-26 Seed Health, Inc. Methods and compositions for honey bee health
CN109232690A (zh) * 2018-09-10 2019-01-18 南方医科大学南方医院 一种正电子显像剂标准品前体及其制备方法
RU2712497C1 (ru) * 2018-11-26 2020-01-29 Автономная некоммерческая образовательная организация высшего образования Сколковский институт науки и технологий Средство разрезания ДНК на основе Cas9 белка из биотехнологически значимой бактерии Clostridium cellulolyticum
SG11202106209RA (en) 2018-12-19 2021-07-29 Univ Leland Stanford Junior Bifunctional molecules for lysosomal targeting and related compositions and methods
IL294515A (en) 2020-01-31 2022-09-01 Avilar Therapeutics Inc Compounds bind asgpr to degrade extracellular proteins
IL298406A (en) 2020-05-22 2023-01-01 Wave Life Sciences Ltd Double stranded oligonucleotide compositions and methods relating thereto
US20240309084A1 (en) 2021-01-19 2024-09-19 Novartis Ag Degradation of extracellular targets
KR20240006496A (ko) * 2021-02-08 2024-01-15 에멘도바이오 인코포레이티드 Omni 90-99, 101, 104-110, 114, 116, 118-123, 125, 126, 128, 129, 및 131-138 crispr 뉴클레아제
WO2022192478A1 (en) * 2021-03-10 2022-09-15 Biohaven Therapeutics Ltd. Bifunctional degraders of galactose-deficient immunoglobulins
JP2024517812A (ja) 2021-05-03 2024-04-23 アヴィラー セラピューティクス インコーポレイテッド 免疫グロブリン及びその他のタンパク質を分解する強力なａｓｇｐｒ結合性化合物
WO2023288033A1 (en) 2021-07-14 2023-01-19 Lycia Therapeutics, Inc. Asgpr cell surface receptor binding compounds and conjugates
WO2023009554A1 (en) * 2021-07-26 2023-02-02 Avilar Therapeutics, Inc. Methods to reduce adverse effects of gene or biologics therapy
EP4392430A1 (en) * 2021-08-27 2024-07-03 Yale University Molecular degraders of extracellular proteins
WO2024167900A2 (en) * 2023-02-06 2024-08-15 Biohaven Therapeutics Ltd. Bifunctional molecules to target degradation of tumor necrosis factor
WO2024229005A2 (en) * 2023-04-30 2024-11-07 Biohaven Therapeutics Ltd. Asgpr binders and compositions and methods thereof
GB202311324D0 (en) 2023-07-24 2023-09-06 Astrazeneca Ab Multivalent cargo-carrying complexes and uses thereof
US20250051771A1 (en) 2023-07-24 2025-02-13 Astrazeneca Ab Multivalent cargo-carrying complexes and uses thereof
GB202311334D0 (en) 2023-07-24 2023-09-06 Astrazeneca Ab Multivalent cargo-carrying complexes and uses thereof
AU2024369609A1 (en) 2023-10-31 2025-12-11 Korro Bio, Inc. Oligonucleotides comprising phosphoramidate internucleotide linkages
CN120381530A (zh) * 2024-01-26 2025-07-29 浙江养生堂天然药物研究所有限公司 偶联物及其制备方法和用途

Family Cites Families (32)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JPS58121243A (ja) * 1982-01-12 1983-07-19 Sumitomo Chem Co Ltd 新規ビシクロオクタン誘導体及びその製造法
US4816567A (en) 1983-04-08 1989-03-28 Genentech, Inc. Recombinant immunoglobin preparations
US5104797A (en) 1988-05-05 1992-04-14 The Procter & Gamble Company Process for preparing 5-c-hydroxymethyl aldohexose-based compounds
US5064672A (en) * 1988-05-05 1991-11-12 The Procter & Gamble Company Functional sugar substitutes with reduced calories
US5041541A (en) * 1988-05-05 1991-08-20 The Procter & Gamble Company Functional sugar substituted with reduced calories
WO1991009537A1 (en) 1989-12-21 1991-07-11 The Procter & Gamble Company Food compositions containing reduced calorie fats and reduced calorie sugars
ES2114948T3 (es) 1991-10-04 1998-06-16 Procter & Gamble Compuestos disminuidores del colesterol y procedimiento para prepararlos.
JPH09506594A (ja) * 1993-12-07 1997-06-30 ネオルクス コーポレーション プレターゲティング方法及び化合物
EP1432724A4 (en) 2002-02-20 2006-02-01 Sirna Therapeutics Inc INTERFERENCE MEDIATION INHIBITION OF GENE RNA FROM MAP KINASE
WO2006022325A1 (ja) * 2004-08-26 2006-03-02 Nippon Shinyaku Co., Ltd. ガラクトース誘導体、薬物担体及び医薬組成物
JP2008540504A (ja) 2005-05-10 2008-11-20 グラクソスミスクライン・イストラジヴァッキ・センタル・ザグレブ・ドルズバ・ゼー・オメイェノ・オドゴヴォルノスティオ 細菌感染症の処置に有用な４’’アミノ結合マクロライド
US7964636B2 (en) 2005-11-07 2011-06-21 University Of South Carolina Synthesis and use of novel inhibitors and inactivators of protein arginine deiminases
US7919598B2 (en) 2006-06-28 2011-04-05 Bristol-Myers Squibb Company Crystal structures of SGLT2 inhibitors and processes for preparing same
AU2009286380B2 (en) * 2008-08-28 2011-09-15 Pfizer Inc. Dioxa-bicyclo[3.2.1.]octane-2,3,4-triol derivatives
JP5696156B2 (ja) * 2009-11-02 2015-04-08 ファイザー・インク ジオキサ−ビシクロ［３．２．１］オクタン−２，３，４−トリオール誘導体
CN102372722A (zh) 2010-08-10 2012-03-14 江苏恒瑞医药股份有限公司 C-芳基葡萄糖苷衍生物、其制备方法及其在医药上的应用
WO2012041898A1 (en) 2010-09-29 2012-04-05 Celon Pharma Sp. Z O.O. Combination of sglt2 inhibitor and a sugar compound for the treatment of diabetes
JP2014517032A (ja) 2011-06-13 2014-07-17 パナセア バイオテック リミテッド 新規のｓｇｌｔ阻害剤
US9018249B2 (en) 2011-09-13 2015-04-28 Panacea Biotec Limited SGLT inhibitors
US20160046961A1 (en) 2012-05-25 2016-02-18 Emmanuelle Charpentier Methods and Compositions for RNA-Directed Target DNA Modification and For RNA-Directed Modulation of Transcription
CN103570657A (zh) 2012-07-19 2014-02-12 天津药物研究院 一类含偕二甲基的苯基c-葡萄糖苷衍生物、其制备方法和用途
WO2014018671A1 (en) * 2012-07-24 2014-01-30 Regents Of The University Of Minnesota Therapeutic compounds for the treatment of cancer
AR092924A1 (es) 2012-10-09 2015-05-06 Sanofi Sa Derivados de pirrolidinona como moduladores de gpr119 para el tratamiento de diabetes, obesidad, dislipidemia y trastornos relacionados
CN103772449B (zh) 2012-10-26 2017-12-26 上海阳帆医药科技有限公司 C‑芳基葡萄糖苷衍生物及其制备方法与用途
US20140189896A1 (en) 2012-12-12 2014-07-03 Feng Zhang Crispr-cas component systems, methods and compositions for sequence manipulation
CN103864737B (zh) 2012-12-17 2016-08-17 天津药物研究院 含脱氧葡萄糖结构的苯基c-葡萄糖苷衍生物及其制备方法和用途
WO2014094544A1 (zh) 2012-12-17 2014-06-26 天津药物研究院 含脱氧葡萄糖结构的苯基c-葡萄糖苷衍生物及其制备方法和用途
WO2014159151A1 (en) 2013-03-14 2014-10-02 Msd International Gmbh Methods for preparing sglt2 inhibitors
FI2981269T3 (fi) 2013-04-04 2023-09-27 Boehringer Ingelheim Vetmedica Gmbh Aineenvaihduntahäiriöiden hoito hevoseläimillä
DK3145934T5 (da) 2014-05-19 2020-11-30 Pfizer Substituerede-6,8-dioxabicyclo[3.2.1]octan-2,3-diol-forbindelser som ASGPR-targeteringsmidler
CN104031098A (zh) 2014-06-21 2014-09-10 李友香 降糖药物
CN104017031A (zh) 2014-06-21 2014-09-03 李友香 降血糖药物和组合物

Also Published As

Publication number Publication date
US9340553B2 (en) 2016-05-17
TWI579286B (zh) 2017-04-21
US10376531B2 (en) 2019-08-13
BR112016026809A2 (pt) 2017-12-12
CA2891717A1 (en) 2015-11-19
WO2015177668A1 (en) 2015-11-26
KR102149572B1 (ko) 2020-08-28
US20190321382A1 (en) 2019-10-24
US20170165284A1 (en) 2017-06-15
AU2015262993B2 (en) 2019-11-07
JP6663889B2 (ja) 2020-03-13
EP3145934B1 (en) 2020-11-11
JP2017515865A (ja) 2017-06-15
RU2696490C2 (ru) 2019-08-02
TW201605864A (zh) 2016-02-16
SA516380328B1 (ar) 2021-06-24
DK3145934T5 (da) 2020-11-30
CN106459120A (zh) 2017-02-22
JP2018035142A (ja) 2018-03-08
AU2015262993A1 (en) 2016-11-10
PL3145934T3 (pl) 2021-08-16
US9617293B2 (en) 2017-04-11
PT3145934T (pt) 2020-12-31
DK3145934T3 (da) 2020-11-23
MX2016015199A (es) 2017-02-28
MY181586A (en) 2020-12-29
US10813942B2 (en) 2020-10-27
IL248667A0 (en) 2017-01-31
RU2016142704A (ru) 2018-06-20
US20180296585A1 (en) 2018-10-18
HUE052146T2 (hu) 2021-04-28
US20160207953A1 (en) 2016-07-21
PH12016502304A1 (en) 2017-02-13
JP6193513B2 (ja) 2017-09-06
ES2841400T3 (es) 2021-07-08
NZ725600A (en) 2023-09-29
US20150329555A1 (en) 2015-11-19
IL248667B (en) 2021-02-28
RU2016142704A3 (es) 2018-06-20
KR20170004005A (ko) 2017-01-10
CA2891717C (en) 2023-09-05
SG11201608936UA (en) 2016-12-29
EP3145934A1 (en) 2017-03-29
UY36126A (es) 2016-01-08
US10039778B2 (en) 2018-08-07
SI3145934T1 (sl) 2021-04-30
MX381383B (es) 2025-03-12

Similar Documents

Publication Publication Date Title
PE20170024A1 (es) Compuestos de 6,8-dioxabiciclo [3.2.1] octano-2,3-diol sustituidos como agentes de direccionamiento al asgpr
CL2011002706A1 (es) Compuestos derivados de 4-(1,3-oxazol-2-il)-1h-indazol; composicion farmaceutica que los comprende; y sus usos en el tratamiento de enfermedades tales como epoc, autoinmunes, asma, entre otras.
SV2011003903A (es) Aminotetrahidropiranos como inhibidores de dipeptidil peptidasa iv para el tratamiento o prevencion de diabetes
CO6321265A2 (es) Compuestos de 2-amido-3-metil pirrolo pirimidinona fenilo -sustituidos como inhibidores bace-1 composiciones y su uso
AR081058A1 (es) Derivados de arilmetoxi isoindolina, composiciones que los comprenden y su uso en el tratamiento del cancer.
AR085960A1 (es) 1,3-oxazinas como inhibidores de la bace1 y/o de la bace2
AR080197A1 (es) Compuestos de pirrolopirimidina deuterada como inhibidores de la cdk 4/6
BR122013028005B8 (pt) compostos de ciclopentanos de pirimidila hidroxilados e metoxilados, composição farmacêutica, kit e forma de dosagem oral compreendendo os referidos compostos, uso das referidas composições, bem como processo de preparação dos referidos compostos
PA8785801A1 (es) Compuestos heterocìclicos
AR051326A1 (es) Pirazolobenzodiazepinas disustituidas
PE20161218A1 (es) (2s)-n-[(1s)-1-ciano-2-feniletil]-1,4-oxazepan-2-carboxamidas como inhibidores de dipeptidil peptidasa 1
AR075729A1 (es) Derivados de benzofuranilo, composiciones farmaceuticas que los contienen y uso de los mismos en el tratamiento de la obesidad y/o diabetes.
UY30498A1 (es) Nueva clase de compuestos de benzimidazolilo, sus sales, composiciones farmacéuticas conteniéndolos y aplicaciones
BR112014026176A2 (pt) dipiridilaminas substituídas e usos das mesmas
AR074453A1 (es) Compuestos 4-(azacicloalquil ) benceno-1,3-diol, como inhibidores de la tirosinasa y su uso en medicina humana y tambien en cosmetica
AR074359A1 (es) Compuestos heterociclicos sustituidos como moduladores de canales ionicos
MA37886B1 (fr) Nouvelles pyridinones bicycliques
CR9721A (es) Compuestos de carbamato para utilizar en el tratamiento de desordenes neurodegenerativos
BR112012028445A2 (pt) compostos de heteroarila bicíclica como moduladores de gpr119
DOP2011000134A (es) Lactamas como inhibidores de beta secretasa
BR112015008717A2 (pt) composto, composição farmacêutica, método de tratar diabetes do tipo ii, uso do composto de fórmula (i), medicação para o tratamento de diabetes do tipo ii
UY33278A (es) Pirimidinas sustituidas como antagonistas del receptor de la protaglandina d2
PH12012501853A1 (en) Pyrimidinylpiperidinyloxypyridinone analogues as gpr119 modulators
UY29184A1 (es) Derivados de sulfonilbencimidazol
ECSP11011124A (es) Antagonistas de 4-azetidinil-1-heteroaril-ciclohexanol de ccr2