RU2696490C2 - Замещенные-6,8-диоксабицикло[3.2.1.]октан-2,3-диольные соединения в качестве агентов, нацеленных на ASGPR - Google Patents

Замещенные-6,8-диоксабицикло[3.2.1.]октан-2,3-диольные соединения в качестве агентов, нацеленных на ASGPR Download PDF

Info

Publication number
RU2696490C2
RU2696490C2 RU2016142704A RU2016142704A RU2696490C2 RU 2696490 C2 RU2696490 C2 RU 2696490C2 RU 2016142704 A RU2016142704 A RU 2016142704A RU 2016142704 A RU2016142704 A RU 2016142704A RU 2696490 C2 RU2696490 C2 RU 2696490C2
Authority
RU
Russia
Prior art keywords
dioxabicyclo
mmol
dihydroxy
methanol
oct
Prior art date
Application number
RU2016142704A
Other languages
English (en)
Russian (ru)
Other versions
RU2016142704A3 (enExample
RU2016142704A (ru
Inventor
Винсен Маситти
Бенджамин ТУМА
Спирос Лирас
Original Assignee
Пфайзер Инк.
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 Пфайзер Инк. filed Critical Пфайзер Инк.
Publication of RU2016142704A3 publication Critical patent/RU2016142704A3/ru
Publication of RU2016142704A publication Critical patent/RU2016142704A/ru
Application granted granted Critical
Publication of RU2696490C2 publication Critical patent/RU2696490C2/ru

Links

Images

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
    • A61K31/70—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
    • C07H13/02—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
    • 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)
RU2016142704A 2014-05-19 2015-05-05 Замещенные-6,8-диоксабицикло[3.2.1.]октан-2,3-диольные соединения в качестве агентов, нацеленных на ASGPR RU2696490C2 (ru)

Applications Claiming Priority (7)

Application Number Priority Date Filing Date Title
US201462000211P 2014-05-19 2014-05-19
US62/000,211 2014-05-19
US201462001540P 2014-05-21 2014-05-21
US62/001,540 2014-05-21
US201562139254P 2015-03-27 2015-03-27
US62/139,254 2015-03-27
PCT/IB2015/053282 WO2015177668A1 (en) 2014-05-19 2015-05-05 Substituted-6,8-dioxabicyclo[3.2.1]octane-2,3-diol compounds as targeting agents of asgpr

Publications (3)

Publication Number Publication Date
RU2016142704A3 RU2016142704A3 (enExample) 2018-06-20
RU2016142704A RU2016142704A (ru) 2018-06-20
RU2696490C2 true RU2696490C2 (ru) 2019-08-02

Family

ID=53200246

Family Applications (1)

Application Number Title Priority Date Filing Date
RU2016142704A RU2696490C2 (ru) 2014-05-19 2015-05-05 Замещенные-6,8-диоксабицикло[3.2.1.]октан-2,3-диольные соединения в качестве агентов, нацеленных на ASGPR

Country Status (26)

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

Families Citing this family (52)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
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
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
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
US11273187B2 (en) 2015-11-30 2022-03-15 Joseph E. Kovarik Method and system for reducing the likelihood of developing depression in an individual
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
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
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
US12257272B2 (en) 2015-12-24 2025-03-25 Seed Health, Inc. Method and system for reducing the likelihood of developing depression in an individual
US11419903B2 (en) 2015-11-30 2022-08-23 Seed Health, Inc. Method and system for reducing the likelihood of osteoporosis
US11844720B2 (en) 2011-02-04 2023-12-19 Seed Health, Inc. Method and system to reduce the likelihood of dental caries and halitosis
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
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
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
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
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
US11833177B2 (en) 2013-12-20 2023-12-05 Seed Health, Inc. Probiotic to enhance an individual's skin microbiome
US12005085B2 (en) 2013-12-20 2024-06-11 Seed Health, Inc. Probiotic method and composition for maintaining a healthy vaginal microbiome
US11969445B2 (en) 2013-12-20 2024-04-30 Seed Health, Inc. Probiotic composition and method for controlling excess weight, obesity, NAFLD and NASH
US11826388B2 (en) 2013-12-20 2023-11-28 Seed Health, Inc. Topical application of Lactobacillus crispatus to ameliorate barrier damage and inflammation
US12246043B2 (en) 2013-12-20 2025-03-11 Seed Health, Inc. Topical application to treat acne vulgaris
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
US11998574B2 (en) 2013-12-20 2024-06-04 Seed Health, Inc. Method and system for modulating an individual's skin microbiome
JP6193513B2 (ja) 2014-05-19 2017-09-06 ファイザー・インク Ａｓｇｐｒ標的化剤としての置換６，８−ジオキサビシクロ［３．２．１］オクタン−２，３−ジオール化合物
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
US12485178B2 (en) 2018-04-09 2025-12-02 Yale University Bifunctional small molecules to target the selective degradation of circulating proteins
US20230097887A1 (en) 2018-04-09 2023-03-30 Yale University Bi-functional Molecules to Degrade Circulating Proteins
CA3134765A1 (en) * 2018-04-09 2019-10-17 Yale University Bi-functional molecules to degrade circulating proteins
WO2019199634A1 (en) * 2018-04-09 2019-10-17 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
BR112021012113A2 (pt) 2018-12-19 2021-09-08 The Board Of Trustees Of The Leland Stanford Junior University Moléculas bifuncionais para direcionamento lisossomal e composições e métodos relacionados
JP2023511756A (ja) 2020-01-31 2023-03-22 アヴィラー セラピューティクス インコーポレイテッド 細胞外タンパク質を分解するａｓｇｐｒ結合性化合物
EP4153747A2 (en) 2020-05-22 2023-03-29 Wave Life Sciences Ltd. Double stranded oligonucleotide compositions and methods relating thereto
JP2024503687A (ja) 2021-01-19 2024-01-26 ノバルティス アーゲー 細胞外標的の分解
US20240425885A1 (en) * 2021-02-08 2024-12-26 Emendobio Inc. OMNI 90-99, 101, 104-110, 114, 116, 118-123, 125, 126, 128, 129, and 131-138 CRISPR NUCLEASE
MX2023010424A (es) * 2021-03-10 2023-09-18 Biohaven Therapeutics Ltd Degradadores bifuncionales de inmunoglobulina deficientes en galactosa.
EP4334360A2 (en) 2021-05-03 2024-03-13 Avilar Therapeutics, Inc. Potent asgpr-binding compounds for the degradation of immunoglobulins and other proteins
CN117957020A (zh) 2021-07-14 2024-04-30 利西亚治疗公司 Asgpr细胞表面受体结合化合物和缀合物
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
GB202311334D0 (en) 2023-07-24 2023-09-06 Astrazeneca Ab Multivalent cargo-carrying complexes and uses thereof
GB202311324D0 (en) 2023-07-24 2023-09-06 Astrazeneca Ab Multivalent cargo-carrying complexes and uses thereof
WO2025021831A1 (en) 2023-07-24 2025-01-30 Astrazeneca Ab Multivalent cargo-carrying complexes and uses thereof
WO2025096809A1 (en) 2023-10-31 2025-05-08 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

Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP0341062A2 (en) * 1988-05-05 1989-11-08 The Procter & Gamble Company Functional sugar substitutes with reduced calories
WO2010023594A1 (en) * 2008-08-28 2010-03-04 Pfizer Inc. Dioxa-bicyclo[3.2.1.]octane-2,3,4-triol derivatives
EA201290267A1 (ru) * 2009-11-02 2012-12-28 Пфайзер Инк. Производные диоксабицикло[3.2.1]октан-2,3,4-триола

Family Cites Families (29)

* 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
WO1991009537A1 (en) 1989-12-21 1991-07-11 The Procter & Gamble Company Food compositions containing reduced calorie fats and reduced calorie sugars
JPH06511250A (ja) 1991-10-04 1994-12-15 ザ、プロクター、エンド、ギャンブル、カンパニー コレステロール低下化合物及びそれらの製造方法
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
AU2003207708A1 (en) 2002-02-20 2003-09-09 Sirna Therapeutics, Inc. Rna interference mediated inhibition of map kinase genes
JP5087924B2 (ja) * 2004-08-26 2012-12-05 日本新薬株式会社 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
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
US20140228303A1 (en) 2011-06-13 2014-08-14 Panacea Biotec Ltd Novel sglt inhibitors
WO2013038429A2 (en) 2011-09-13 2013-03-21 Panacea Biotec Ltd. Novel 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
CA2894668A1 (en) 2012-12-12 2014-06-19 The Broad Institute, Inc. Crispr-cas systems and methods for altering expression of gene products in eukaryotic cells
JP5944593B2 (ja) 2012-12-17 2016-07-05 ティエンジン インスティテュート オブ ファーマシューティカル リサーチ デオキシグルコース構造を有するフェニルｃ−グルコシド誘導体、その調製方法および使用方法
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
ES2740299T3 (es) 2013-03-14 2020-02-05 Msd Int Gmbh Métodos para preparar inhibidores de SGLT2
EP2981269B9 (en) 2013-04-04 2023-12-06 Boehringer Ingelheim Vetmedica GmbH Treatment of metabolic disorders in equine animals
JP6193513B2 (ja) * 2014-05-19 2017-09-06 ファイザー・インク Ａｓｇｐｒ標的化剤としての置換６，８−ジオキサビシクロ［３．２．１］オクタン−２，３−ジオール化合物
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

Patent Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP0341062A2 (en) * 1988-05-05 1989-11-08 The Procter & Gamble Company Functional sugar substitutes with reduced calories
WO2010023594A1 (en) * 2008-08-28 2010-03-04 Pfizer Inc. Dioxa-bicyclo[3.2.1.]octane-2,3,4-triol derivatives
EA201290267A1 (ru) * 2009-11-02 2012-12-28 Пфайзер Инк. Производные диоксабицикло[3.2.1]октан-2,3,4-триола

Non-Patent Citations (3)

* Cited by examiner, † Cited by third party
Title
J. R. H. Plet et al. "Thieme Chemistry Journal Awardees - Where Are They Now? Approaches to Tagetitoxin and its Decarboxy Analogue from d-Glucose" SYNLETT, N20, 2009, 3258-3262, соед. 27. *
J. R. H. Plet et al. "Thieme Chemistry Journal Awardees - Where Are They Now? Approaches to Tagetitoxin and its Decarboxy Analogue from d-Glucose" SYNLETT, N20, 2009, 3258-3262, соед. 27. S. K. Mamidyala et al. "Glucomimetic Ligands for the Human Asiloglycoprotein receptor" JOURNAL OF THE AMERICAN CHEMICAL SOCIETY, vol.134, N4, 2012, 1978-1981. *
S. K. Mamidyala et al. "Glucomimetic Ligands for the Human Asiloglycoprotein receptor" JOURNAL OF THE AMERICAN CHEMICAL SOCIETY, vol.134, N4, 2012, 1978-1981. *

Also Published As

Publication number Publication date
AU2015262993B2 (en) 2019-11-07
IL248667B (en) 2021-02-28
CA2891717C (en) 2023-09-05
RU2016142704A3 (enExample) 2018-06-20
US10813942B2 (en) 2020-10-27
US9340553B2 (en) 2016-05-17
WO2015177668A1 (en) 2015-11-26
US20190321382A1 (en) 2019-10-24
CN106459120A (zh) 2017-02-22
AU2015262993A1 (en) 2016-11-10
JP2017515865A (ja) 2017-06-15
JP6663889B2 (ja) 2020-03-13
PH12016502304A1 (en) 2017-02-13
IL248667A0 (en) 2017-01-31
BR112016026809A2 (pt) 2017-12-12
ES2841400T3 (es) 2021-07-08
US20180296585A1 (en) 2018-10-18
JP6193513B2 (ja) 2017-09-06
SA516380328B1 (ar) 2021-06-24
PE20170024A1 (es) 2017-03-17
CA2891717A1 (en) 2015-11-19
JP2018035142A (ja) 2018-03-08
US9617293B2 (en) 2017-04-11
MX381383B (es) 2025-03-12
SG11201608936UA (en) 2016-12-29
EP3145934A1 (en) 2017-03-29
US10039778B2 (en) 2018-08-07
DK3145934T5 (da) 2020-11-30
KR20170004005A (ko) 2017-01-10
US20160207953A1 (en) 2016-07-21
PL3145934T3 (pl) 2021-08-16
TW201605864A (zh) 2016-02-16
US20170165284A1 (en) 2017-06-15
US20150329555A1 (en) 2015-11-19
DK3145934T3 (da) 2020-11-23
TWI579286B (zh) 2017-04-21
HUE052146T2 (hu) 2021-04-28
KR102149572B1 (ko) 2020-08-28
EP3145934B1 (en) 2020-11-11
SI3145934T1 (sl) 2021-04-30
UY36126A (es) 2016-01-08
US10376531B2 (en) 2019-08-13
MY181586A (en) 2020-12-29
MX2016015199A (es) 2017-02-28
PT3145934T (pt) 2020-12-31
RU2016142704A (ru) 2018-06-20
NZ725600A (en) 2023-09-29

Similar Documents

Publication Publication Date Title
RU2696490C2 (ru) Замещенные-6,8-диоксабицикло[3.2.1.]октан-2,3-диольные соединения в качестве агентов, нацеленных на ASGPR
US12168023B2 (en) Inhibitors of adenosine 5′-nucleotidase
US11267845B2 (en) Inhibitors of CD73-mediated immunosuppression
US12134631B2 (en) Hydrophilic linkers for antibody drug conjugates
JP2020143062A (ja) 低細胞透過性を有するＢｃｌ−ｘＬ阻害性化合物およびこれを含む抗体薬物コンジュゲート
KR20240043823A (ko) 링커, 약물 링커 및 그의 접합체, 및 그의 사용 방법
AU2020279979A1 (en) Mcl-1 inhibitor antibody-drug conjugates and methods of use
KR102722886B1 (ko) 신규한 펩티드 링커 및 크립토피신 콘쥬게이트, 이들의 제조 및 이들의 치료적 용도
KR20240150809A (ko) 비스-옥타하이드로페난트렌 카복스아미드 및 이의 단백질 접합체
JP2020500148A (ja) 新規細胞傷害性剤およびそのコンジュゲート
US20240408223A1 (en) Hydrophilic linkers for antibody drug conjugates
HK1232545A1 (en) Substituted-6,8-dioxabicyclo[3.2.1]octane-2,3-diol compounds as targeting agents of asgpr
AU2024261051A1 (en) Antibody-drug conjugate compounds, and methods of use and treatment
JP2025183333A (ja) Ｍｃｌ－１阻害剤抗体－薬物コンジュゲートおよび使用方法
CN121002040A (zh) 细胞毒性化合物
CN120513102A (zh) 一种抗体药物偶联物及其制备方法和用途