EA031609B1 - Соединения и композиции для стимулирования хондрогенеза - Google Patents

Соединения и композиции для стимулирования хондрогенеза Download PDF

Info

Publication number
EA031609B1
EA031609B1 EA201692292A EA201692292A EA031609B1 EA 031609 B1 EA031609 B1 EA 031609B1 EA 201692292 A EA201692292 A EA 201692292A EA 201692292 A EA201692292 A EA 201692292A EA 031609 B1 EA031609 B1 EA 031609B1
Authority
EA
Eurasian Patent Office
Prior art keywords
carboxamide
heptane
oxabicyclo
pyridin
biphenyl
Prior art date
Application number
EA201692292A
Other languages
English (en)
Russian (ru)
Other versions
EA201692292A1 (ru
Inventor
Ха-Соон Чои
Джеймс Пол Лэджинесс
Сриниваса Редди Натала
Бао Нгуйен
Ханк Майкл Джеймс Петрасси
Чжичэнь Ван
Original Assignee
Новартис Аг
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 Новартис Аг filed Critical Новартис Аг
Publication of EA201692292A1 publication Critical patent/EA201692292A1/ru
Publication of EA031609B1 publication Critical patent/EA031609B1/ru

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D493/00Heterocyclic compounds containing oxygen atoms as the only ring hetero atoms in the condensed system
    • C07D493/02Heterocyclic compounds containing oxygen atoms as the only ring hetero atoms in the condensed system in which the condensed system contains two hetero rings
    • C07D493/08Bridged systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/335Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
    • A61K31/34Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having five-membered rings with one oxygen as the only ring hetero atom, e.g. isosorbide
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/335Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
    • A61K31/35Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having six-membered rings with one oxygen as the only ring hetero atom
    • A61K31/351Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having six-membered rings with one oxygen as the only ring hetero atom not condensed with another ring
    • 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
    • A61K31/41Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/4151,2-Diazoles
    • A61K31/41551,2-Diazoles non condensed and containing further heterocyclic rings
    • 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
    • A61K31/41Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/4151,2-Diazoles
    • A61K31/4161,2-Diazoles condensed with carbocyclic ring systems, e.g. indazole
    • 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
    • A61K31/41Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/4245Oxadiazoles
    • 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
    • A61K31/4427Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/443Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with oxygen as a ring hetero atom
    • 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
    • A61K31/4427Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/4433Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with oxygen as a ring hetero atom
    • 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
    • A61K31/4427Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/4439Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
    • 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
    • A61K31/4427Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/444Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring heteroatom, e.g. amrinone
    • 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
    • A61K31/4525Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a five-membered ring with oxygen as a ring hetero atom
    • 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
    • A61K31/495Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/4965Non-condensed pyrazines
    • A61K31/497Non-condensed pyrazines containing further heterocyclic rings
    • 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
    • A61K31/495Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/506Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
    • 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
    • A61LMETHODS OR APPARATUS FOR STERILISING MATERIALS OR OBJECTS IN GENERAL; DISINFECTION, STERILISATION OR DEODORISATION OF AIR; CHEMICAL ASPECTS OF BANDAGES, DRESSINGS, ABSORBENT PADS OR SURGICAL ARTICLES; MATERIALS FOR BANDAGES, DRESSINGS, ABSORBENT PADS OR SURGICAL ARTICLES
    • A61L27/00Materials for grafts or prostheses or for coating grafts or prostheses
    • A61L27/50Materials characterised by their function or physical properties, e.g. injectable or lubricating compositions, shape-memory materials, surface modified materials
    • A61L27/54Biologically active materials, e.g. therapeutic substances
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • A61P19/02Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • A61P19/08Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • A61P19/10Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease for osteoporosis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D491/00Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
    • C07D491/12Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains three hetero rings
    • C07D491/18Bridged systems
    • CCHEMISTRY; METALLURGY
    • C12BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
    • C12NMICROORGANISMS OR ENZYMES; COMPOSITIONS THEREOF; PROPAGATING, PRESERVING, OR MAINTAINING MICROORGANISMS; MUTATION OR GENETIC ENGINEERING; CULTURE MEDIA
    • C12N5/00Undifferentiated human, animal or plant cells, e.g. cell lines; Tissues; Cultivation or maintenance thereof; Culture media therefor
    • C12N5/06Animal cells or tissues; Human cells or tissues
    • C12N5/0602Vertebrate cells
    • C12N5/0652Cells of skeletal and connective tissues; Mesenchyme
    • C12N5/0655Chondrocytes; Cartilage
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61LMETHODS OR APPARATUS FOR STERILISING MATERIALS OR OBJECTS IN GENERAL; DISINFECTION, STERILISATION OR DEODORISATION OF AIR; CHEMICAL ASPECTS OF BANDAGES, DRESSINGS, ABSORBENT PADS OR SURGICAL ARTICLES; MATERIALS FOR BANDAGES, DRESSINGS, ABSORBENT PADS OR SURGICAL ARTICLES
    • A61L2300/00Biologically active materials used in bandages, wound dressings, absorbent pads or medical devices
    • A61L2300/40Biologically active materials used in bandages, wound dressings, absorbent pads or medical devices characterised by a specific therapeutic activity or mode of action
    • A61L2300/412Tissue-regenerating or healing or proliferative agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61LMETHODS OR APPARATUS FOR STERILISING MATERIALS OR OBJECTS IN GENERAL; DISINFECTION, STERILISATION OR DEODORISATION OF AIR; CHEMICAL ASPECTS OF BANDAGES, DRESSINGS, ABSORBENT PADS OR SURGICAL ARTICLES; MATERIALS FOR BANDAGES, DRESSINGS, ABSORBENT PADS OR SURGICAL ARTICLES
    • A61L2430/00Materials or treatment for tissue regeneration
    • A61L2430/06Materials or treatment for tissue regeneration for cartilage reconstruction, e.g. meniscus
    • CCHEMISTRY; METALLURGY
    • C12BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
    • C12NMICROORGANISMS OR ENZYMES; COMPOSITIONS THEREOF; PROPAGATING, PRESERVING, OR MAINTAINING MICROORGANISMS; MUTATION OR GENETIC ENGINEERING; CULTURE MEDIA
    • C12N2501/00Active agents used in cell culture processes, e.g. differentation
    • C12N2501/999Small molecules not provided for elsewhere
    • CCHEMISTRY; METALLURGY
    • C12BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
    • C12NMICROORGANISMS OR ENZYMES; COMPOSITIONS THEREOF; PROPAGATING, PRESERVING, OR MAINTAINING MICROORGANISMS; MUTATION OR GENETIC ENGINEERING; CULTURE MEDIA
    • C12N2506/00Differentiation of animal cells from one lineage to another; Differentiation of pluripotent cells
    • C12N2506/13Differentiation of animal cells from one lineage to another; Differentiation of pluripotent cells from connective tissue cells, from mesenchymal cells
    • C12N2506/1346Differentiation of animal cells from one lineage to another; Differentiation of pluripotent cells from connective tissue cells, from mesenchymal cells from mesenchymal stem cells
    • YGENERAL 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
    • Y02TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
    • Y02ATECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE
    • Y02A50/00TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE in human health protection, e.g. against extreme weather
    • Y02A50/30Against vector-borne diseases, e.g. mosquito-borne, fly-borne, tick-borne or waterborne diseases whose impact is exacerbated by climate change

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Organic Chemistry (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Rheumatology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Biomedical Technology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Wood Science & Technology (AREA)
  • Biotechnology (AREA)
  • Zoology (AREA)
  • Genetics & Genomics (AREA)
  • Biochemistry (AREA)
  • Oral & Maxillofacial Surgery (AREA)
  • Cell Biology (AREA)
  • Transplantation (AREA)
  • General Engineering & Computer Science (AREA)
  • Molecular Biology (AREA)
  • Dermatology (AREA)
  • Microbiology (AREA)
  • Immunology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines Containing Material From Animals Or Micro-Organisms (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
EA201692292A 2014-05-13 2015-05-12 Соединения и композиции для стимулирования хондрогенеза EA031609B1 (ru)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US201461992815P 2014-05-13 2014-05-13
PCT/US2015/030303 WO2015175487A1 (en) 2014-05-13 2015-05-12 Compounds and compositions for inducing chondrogenesis

Publications (2)

Publication Number Publication Date
EA201692292A1 EA201692292A1 (ru) 2017-02-28
EA031609B1 true EA031609B1 (ru) 2019-01-31

Family

ID=53284520

Family Applications (1)

Application Number Title Priority Date Filing Date
EA201692292A EA031609B1 (ru) 2014-05-13 2015-05-12 Соединения и композиции для стимулирования хондрогенеза

Country Status (39)

Country Link
US (6) US9688689B2 (enExample)
EP (2) EP4474384A1 (enExample)
JP (1) JP6479051B2 (enExample)
KR (1) KR102375396B1 (enExample)
CN (1) CN106459076B (enExample)
AP (1) AP2016009502A0 (enExample)
AR (1) AR100418A1 (enExample)
AU (1) AU2015259403B2 (enExample)
BR (1) BR112016025659B1 (enExample)
CA (1) CA2947031C (enExample)
CL (1) CL2016002838A1 (enExample)
CR (1) CR20160528A (enExample)
CU (1) CU24392B1 (enExample)
DK (1) DK3143026T3 (enExample)
EA (1) EA031609B1 (enExample)
ES (1) ES2987439T3 (enExample)
FI (1) FI3143026T3 (enExample)
HR (1) HRP20241236T1 (enExample)
HU (1) HUE067954T2 (enExample)
IL (1) IL248400B (enExample)
JO (1) JO3563B1 (enExample)
LT (1) LT3143026T (enExample)
MA (1) MA39972B1 (enExample)
MX (1) MX377796B (enExample)
MY (1) MY186570A (enExample)
NZ (1) NZ725044A (enExample)
PE (1) PE20161432A1 (enExample)
PH (1) PH12016502005B1 (enExample)
PL (1) PL3143026T3 (enExample)
PT (1) PT3143026T (enExample)
RS (1) RS66122B1 (enExample)
SG (1) SG11201608823RA (enExample)
SI (1) SI3143026T1 (enExample)
SV (1) SV2016005316A (enExample)
TN (1) TN2016000441A1 (enExample)
TW (1) TWI662039B (enExample)
UY (1) UY36118A (enExample)
WO (1) WO2015175487A1 (enExample)
ZA (1) ZA201606929B (enExample)

Families Citing this family (14)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
HK1224172A1 (zh) 2013-03-15 2017-08-18 加州生物医学研究所 用於诱导软骨形成的化合物和方法
US9688689B2 (en) * 2014-05-13 2017-06-27 Novartis Ag Compounds and compositions for inducing chondrogenesis
MX2019005621A (es) * 2016-11-14 2019-08-12 Novartis Ag Metodos y composiciones para el tratamiento del daño del cartilago y la artritis.
WO2018200411A1 (en) * 2017-04-24 2018-11-01 The California Institute For Biomedical Research Methods for inducing chondrogenesis
JOP20190282A1 (ar) 2017-06-09 2019-12-05 Novartis Ag مركبات وتركيبات لحث تكوّن الغضاريف
CN111278410A (zh) * 2017-11-10 2020-06-12 诺华股份有限公司 用于关节内应用的延长释放配制品
KR20210038877A (ko) 2018-07-25 2021-04-08 노파르티스 아게 Nlrp3 인플라마좀 억제제
WO2020115683A1 (en) 2018-12-06 2020-06-11 Novartis Ag 5-hydroxy-7-oxabicyclo[2.2.1]heptane-2-carboxamide derivatives for inducing chondrogenesis for treating joint damage
JP7427665B2 (ja) * 2018-12-06 2024-02-05 ノバルティス アーゲー 関節損傷を治療するための軟骨形成を誘導するための6-ヒドロキシ-8-オキサトリシクロ[3.2.1.02,4]オクタン-2-カルボキサミド誘導体
CN111601789A (zh) * 2018-12-20 2020-08-28 江苏凯迪恩医药科技有限公司 一种含氮杂环化合物、其制备方法及应用
AR119731A1 (es) 2019-05-17 2022-01-05 Novartis Ag Inhibidores del inflamasoma nlrp3
RU2733472C1 (ru) * 2020-02-26 2020-10-01 Федеральное государственное бюджетное учреждение науки Новосибирский институт органической химии им. Н.Н. Ворожцова Сибирского отделения Российской академии наук (НИОХ СО РАН) N-Ацилгидразон фенхона с фрагментом эпоксиизоиндола, используемый в качестве ингибитора репродукции вируса Хантаан
CN114763347B (zh) * 2021-01-15 2024-06-21 华东师范大学 一类用于诱导间充质干细胞向软骨分化的化合物及其应用
UY40374A (es) 2022-08-03 2024-02-15 Novartis Ag Inhibidores de inflamasoma nlrp3

Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4707494A (en) * 1986-08-26 1987-11-17 E. R. Squibb & Sons, Inc. 7-oxabicyclo(2.2.1)heptane compounds useful in the treatment of inflammation
WO2002042310A2 (en) * 2000-11-23 2002-05-30 Bayer Cropscience Ag Oxabicyclo[2.2.1]heptane derivatives as pesticidal agents
CN101628951A (zh) * 2009-08-12 2010-01-20 中国石油天然气股份有限公司 烯烃聚合用固体催化组分及其催化剂
US20100256385A1 (en) * 2009-04-02 2010-10-07 Allergan, Inc. Prostaglandin e receptor antagonists

Family Cites Families (62)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
FR2205274B1 (enExample) 1972-11-02 1976-10-01 Sumitomo Chemical Co
US3925554A (en) 1972-11-30 1975-12-09 Sumitomo Chemical Co Certain 3,5-dichlorophenyl compound used as a plant fungicide
US4687865A (en) 1986-06-04 1987-08-18 E. R. Squibb & Sons, Inc. Process for preparing 7-oxabicycloheptane amino-alcohol intermediates useful in making thromboxane A2 receptor antagonists
JP2984077B2 (ja) 1990-04-19 1999-11-29 塩野義製薬株式会社 スルホニルアミノ置換ビシクロ環系ヒドロキサム酸誘導体
US5126370A (en) 1990-12-24 1992-06-30 E. R. Squibb & Sons, Inc. Anti-thrombotic heterocyclic amido prostaglandin analogs
JPH04275182A (ja) 1991-03-01 1992-09-30 Sankyo Kagaku Kk 感熱転写記録用色素
US5506242A (en) 1993-01-06 1996-04-09 Ciba-Geigy Corporation Arylsufonamido-substituted hydroxamic acids
US5399725A (en) 1993-05-27 1995-03-21 Bristol-Myers Squibb Co. 7-oxabicycloheptane carboxylic acid prostaglandin analog intermediates useful in the preparation of anti-thrombotic and anti-vasospastic compounds and method for preparing same
HUT74949A (en) 1993-09-10 1997-03-28 Cytomed Epibatidine and derivatives thereof as cholinergic receptor agonists and antagonists
US5529925A (en) 1993-12-03 1996-06-25 St. Jude Children's Research Hospital Nucleic acid sequences and fusion proteins present in human t(2;5) lymphoma
US5416106A (en) 1993-12-28 1995-05-16 Allergan, Inc. 7-[carboxyalkyl or alkenyl]-6-[alkyl or alkenyl]3-oxo-2,4-dioxobicyclo-[3.2.1] octane and derivatives thereof
US6017953A (en) 1993-12-28 2000-01-25 Allergan Sales, Inc. Thromboxane ligands
FR2718136B1 (fr) 1994-03-29 1996-06-21 Sanofi Sa Composés aromatiques aminés, procédé pour leur obtention et compositions pharmaceutiques les contenant.
US6447796B1 (en) 1994-05-16 2002-09-10 The United States Of America As Represented By The Secretary Of The Army Sustained release hydrophobic bioactive PLGA microspheres
EP0912170A4 (en) 1996-05-02 2003-04-09 Merck & Co Inc HIV PROTEASE INHIBITORS FOR TREATING AIDS
EP0950059B1 (en) 1997-01-06 2004-08-04 Pfizer Inc. Cyclic sulfone derivatives
MXPA01009073A (es) 1999-03-10 2002-05-06 Phogen Ltd Suministro de acidos nucleicos y proteinas a las celulas.
GB9908021D0 (en) * 1999-04-08 1999-06-02 Lilly Co Eli Pharmaceutical compounds
AU4687500A (en) 1999-04-29 2000-11-17 Allergan Sales, Inc. Thromboxane ligands without blood clotting side effects
JP2003518494A (ja) 1999-12-29 2003-06-10 グラクソ グループ リミテッド アネキシンおよび軟骨ホメオスタシスのモジュレーターに関係する方法と組成物
US20040077605A1 (en) 2001-06-20 2004-04-22 Salvati Mark E. Fused heterocyclic succinimide compounds and analogs thereof, modulators of nuclear hormone receptor function
US20020130430A1 (en) 2000-12-29 2002-09-19 Castor Trevor Percival Methods for making polymer microspheres/nanospheres and encapsulating therapeutic proteins and other products
EP1688412A3 (en) 2001-02-16 2006-08-16 Aventis Pharmaceuticals, Inc. Novel heterocyclic amide derivatives and their use as dopamine D3 receptor ligands
US7060498B1 (en) 2001-11-28 2006-06-13 Genta Salus Llc Polycationic water soluble copolymer and method for transferring polyanionic macromolecules across biological barriers
US7141540B2 (en) 2001-11-30 2006-11-28 Genta Salus Llc Cyclodextrin grafted biocompatible amphilphilic polymer and methods of preparation and use thereof
WO2004078163A2 (en) 2003-02-28 2004-09-16 Transform Pharmaceuticals, Inc. Pharmaceutical co-crystal compositions of drugs such as carbamazepine, celecoxib, olanzapine, itraconazole, topiramate, modafinil, 5-fluorouracil, hydrochlorothiazide, acetaminophen, aspirin, flurbiprofen, phenytoin and ibuprofen
BR0307874A (pt) 2002-02-20 2004-12-28 Upjohn Co Atividade de compostos azabicìclicos com receptor de acetilcolina nicotìnica alfa7
EP1388535A1 (en) 2002-08-07 2004-02-11 Aventis Pharma Deutschland GmbH Acylated arylcycloalkylamines and their use as pharmaceuticals
KR20050105511A (ko) 2003-03-04 2005-11-04 화이자 프로덕츠 인크. 의학적 치료에서 ep2 선택적 수용체 효능제의 용도
EP1661580B1 (en) 2003-07-25 2014-01-08 Ono Pharmaceutical Co., Ltd. Remedy for cartilage-related diseases
JP2005097195A (ja) 2003-09-25 2005-04-14 Institute Of Physical & Chemical Research 医薬組成物
EP1680464A1 (en) 2003-11-07 2006-07-19 Milliken & Company Concentrates of saturated bicyclic dicarboxylate salts as polymer nucleation additives and methods of nucleating thermoplastics
DK2708541T3 (en) 2003-11-13 2015-02-23 Isis Pharmaceuticals Inc 5,6-dihydroxy-isoindole derivatives as linkers for oligomeric solid phase synthesis
US20050203086A1 (en) 2004-03-04 2005-09-15 Pfizer Inc. Methods of treatment using an EP2 selective receptor agonist
EP1792622A1 (en) * 2005-11-11 2007-06-06 GPC Biotech AG Anti-proliferative combination therapy comprising a platinum-based chemotherapeutic agent and EGFR inhibitors or pyrimidine analogues
US7795370B2 (en) 2005-11-15 2010-09-14 Mitsubishi Chemical Corporation Tetracarboxylic acid compound, polyimide thereof, and production method thereof
GB0526240D0 (en) 2005-12-22 2006-02-01 Novartis Ag Organic compounds
US7566797B2 (en) 2006-03-03 2009-07-28 Milliken & Company Metal carboxylate salt nucleating or clarifying agent compounds and related polymer compositions and methods
AU2008214299B2 (en) 2007-02-06 2014-01-09 Lixte Biotechnology, Inc. Oxabicycloheptanes and oxabicycloheptenes, their preparation and use
JP4275182B2 (ja) 2007-11-02 2009-06-10 シャープ株式会社 熱交換器
US8227473B2 (en) 2008-08-01 2012-07-24 Lixte Biotechnology, Inc. Oxabicycloheptanes and oxabicycloheptenes, their preparation and use
CA2730428A1 (en) 2008-08-01 2010-02-04 Lixte Biotechnology, Inc. Methods for regulating cell mitosis by inhibiting serine/threonine phosphatase
EP2318005B1 (en) 2008-08-01 2017-11-01 Lixte Biotechnology, Inc. Neuroprotective agents for the prevention and treatment of neurodegenerative diseases
WO2010017047A1 (en) * 2008-08-05 2010-02-11 Merck & Co., Inc. Therapeutic compounds
WO2010099573A1 (en) 2009-03-03 2010-09-10 Deakin University Dioxolane norbornane / norbornene compounds suitable as antimicrobial agents to treat bacterial infections
HRP20130972T1 (hr) 2009-05-18 2013-11-22 Actelion Pharmaceuticals Ltd. Premošteni derivati spiro [2,4] heptana kao alx-receptori i/ili fprl2-agonisti
PT2453921E (pt) 2009-07-14 2015-09-25 Novartis Ag Diferenciação de células estaminais mesenquimais
JP5478161B2 (ja) 2009-09-03 2014-04-23 株式会社クラレ アクリル酸エステル誘導体およびアルコール誘導体並びにそれらの製造方法
EP2493879B1 (en) 2009-10-28 2014-05-14 Joyant Pharmaceuticals, Inc. Dimeric smac mimetics
US8754059B2 (en) 2010-02-16 2014-06-17 University Of Miami Use of miR-30e to treat vascular lesions
WO2011163502A1 (en) 2010-06-24 2011-12-29 Allergan, Inc. Derivatives of cycloalkyl- and cycloalkenyl-1,2-dicarboxylic acid compounds having formyl peptide receptor like-1 (fprl-1) agonist or antagonist activity
CA2814826C (en) 2010-11-17 2019-02-12 Actelion Pharmaceuticals Ltd Bridged spiro[2.4]heptane ester derivatives
WO2012129562A2 (en) 2011-03-24 2012-09-27 The Scripps Research Institute Compounds and methods for inducing chondrogenesis
WO2012162535A1 (en) 2011-05-24 2012-11-29 Lixte Biotechnology, Inc. Use of phosphatase inhibitors or histone deacetylase inhibitors to treat diseases characterized by loss of protein function
EP2850058B1 (en) 2012-05-16 2016-07-13 Actelion Pharmaceuticals Ltd. 1-(p-tolyl)cyclopropyl substituted bridged spiro[2.4]heptane derivatives as alx receptor agonists
MA37618B1 (fr) 2012-05-16 2017-08-31 Actelion Pharmaceuticals Ltd Dérivés pontés fluorés de spiro[2.4]heptane en tant qu'agonistes de récepteur alx
WO2014005084A1 (en) 2012-06-29 2014-01-03 Lixte Biotechnology, Inc. Oxabicycloheptanes and oxabicycloheptenes for the treatment of diabetes
CA2876703A1 (en) 2012-06-29 2014-01-03 Lixte Biotechnology, Inc. Oxabicycloheptanes and oxabicycloheptenes for the treatment of reperfusion injury
KR20160004299A (ko) 2013-04-09 2016-01-12 릭스트 바이오테크놀로지, 인코포레이티드 옥사바이시클로헵탄류 및 옥사바이시클로헵텐류의 제형
AR096686A1 (es) 2013-06-25 2016-01-27 Actelion Pharmaceuticals Ltd Derivados de espiro[2.4]heptano puenteados sustituidos con difluoroetil-oxazol como agonistas del receptor de alx
AU2014292064B2 (en) 2013-07-18 2018-07-05 Idorsia Pharmaceuticals Ltd Piperazine substituted bridged spiro[2.4]heptane derivatives as alx receptor agonists
US9688689B2 (en) * 2014-05-13 2017-06-27 Novartis Ag Compounds and compositions for inducing chondrogenesis

Patent Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4707494A (en) * 1986-08-26 1987-11-17 E. R. Squibb & Sons, Inc. 7-oxabicyclo(2.2.1)heptane compounds useful in the treatment of inflammation
WO2002042310A2 (en) * 2000-11-23 2002-05-30 Bayer Cropscience Ag Oxabicyclo[2.2.1]heptane derivatives as pesticidal agents
US20100256385A1 (en) * 2009-04-02 2010-10-07 Allergan, Inc. Prostaglandin e receptor antagonists
CN101628951A (zh) * 2009-08-12 2010-01-20 中国石油天然气股份有限公司 烯烃聚合用固体催化组分及其催化剂

Non-Patent Citations (3)

* Cited by examiner, † Cited by third party
Title
CHRISTENSEN, H.S. BOYE, S.V. THINGGAARD, J. SINNING, S. WIBORG, O. SCHIOTT, B. BOLS, M.: "QSAR studies and pharmacophore identification for arylsubstituted cycloalkenecarboxylic acid methyl esters with affinity for the human dopamine transporter", BIOORGANIC & MEDICINAL CHEMISTRY, PERGAMON, GB, vol. 15, no. 15, 8 June 2007 (2007-06-08), GB, pages 5262 - 5274, XP022110128, ISSN: 0968-0896, DOI: 10.1016/j.bmc.2007.05.015 *
SATENDRA SINGH: "Chemistry, Design, and Structure−Activity Relationship of Cocaine Antagonists", CHEMICAL REVIEWS, AMERICAN CHEMICAL SOCIETY, vol. 100, no. 3, 1 March 2000 (2000-03-01), pages 925 - 1024, XP055133125, ISSN: 00092665, DOI: 10.1021/cr9700538 *
SHRIPAD S. BHAGWAT, CANDIDO GUDE, DAVID S COHEN, WARREN LEE, PATRICIA FURNESS, FRANK H CLARKE, FITZGERALD, D J ; DORAN, J ; JACKSO: "Thromboxane receptor antagonism combined with thromboxane synthase inhibition. 1. (.+-.)-(3-Pyridinylbicycloheptyl)alkanoic acids", JOURNAL OF MEDICINAL CHEMISTRY, AMERICAN CHEMICAL SOCIETY, vol. 34, no. 6, 1 June 1991 (1991-06-01), pages 1790 - 1797, XP055204805, ISSN: 00222623, DOI: 10.1021/jm00110a006 *

Also Published As

Publication number Publication date
MX377796B (es) 2025-03-11
TW201623310A (zh) 2016-07-01
SG11201608823RA (en) 2016-11-29
US20200237737A1 (en) 2020-07-30
LT3143026T (lt) 2024-10-10
BR112016025659B1 (pt) 2023-03-07
CU24392B1 (es) 2019-04-04
JP2017519729A (ja) 2017-07-20
ES2987439T3 (es) 2024-11-14
MX2016014854A (es) 2017-02-27
CN106459076A (zh) 2017-02-22
HK1231467A1 (en) 2017-12-22
PT3143026T (pt) 2024-09-27
TWI662039B (zh) 2019-06-11
US12280041B2 (en) 2025-04-22
ZA201606929B (en) 2017-11-29
US20150329554A1 (en) 2015-11-19
PH12016502005A1 (en) 2017-01-09
DK3143026T3 (da) 2024-09-30
BR112016025659A8 (pt) 2021-07-06
EP3143026A1 (en) 2017-03-22
RS66122B1 (sr) 2024-11-29
CU20160169A7 (es) 2017-05-10
CR20160528A (es) 2017-01-02
PH12016502005B1 (en) 2017-01-09
HUE067954T2 (hu) 2024-11-28
AU2015259403A1 (en) 2016-11-03
AP2016009502A0 (en) 2016-10-31
FI3143026T3 (fi) 2024-10-10
TN2016000441A1 (en) 2018-04-04
IL248400B (en) 2019-12-31
CL2016002838A1 (es) 2017-04-28
EP4474384A1 (en) 2024-12-11
CA2947031A1 (en) 2015-11-19
IL248400A0 (en) 2016-11-30
NZ725044A (en) 2019-03-29
US10660881B2 (en) 2020-05-26
CN106459076B (zh) 2019-01-04
MY186570A (en) 2021-07-27
US10188638B2 (en) 2019-01-29
UY36118A (es) 2016-01-08
MA39972B1 (fr) 2024-10-31
US9688689B2 (en) 2017-06-27
US20170239227A1 (en) 2017-08-24
US10383863B2 (en) 2019-08-20
US11510912B2 (en) 2022-11-29
US20190314348A1 (en) 2019-10-17
JP6479051B2 (ja) 2019-03-06
PE20161432A1 (es) 2017-01-08
US20190134012A1 (en) 2019-05-09
US20230112980A1 (en) 2023-04-13
MA39972A (fr) 2015-11-19
PL3143026T3 (pl) 2024-11-12
AU2015259403B2 (en) 2017-07-27
KR102375396B1 (ko) 2022-03-18
EP3143026B1 (en) 2024-07-10
CA2947031C (en) 2023-01-24
AR100418A1 (es) 2016-10-05
WO2015175487A1 (en) 2015-11-19
SI3143026T1 (sl) 2024-10-30
SV2016005316A (es) 2018-06-12
BR112016025659A2 (pt) 2017-08-15
KR20170003563A (ko) 2017-01-09
HRP20241236T1 (hr) 2024-12-06
EA201692292A1 (ru) 2017-02-28
JO3563B1 (ar) 2020-07-05

Similar Documents

Publication Publication Date Title
US12280041B2 (en) Compounds and compositions for inducing chondrogenesis
KR102212923B1 (ko) 키나제 조절을 위한 화합물 및 방법, 및 그에 대한 적응증
JP6523251B2 (ja) C−結合ヘテロシクロアルキル置換ピリミジン類及びそれらの用途
JP2022525749A (ja) Jakキナーゼ阻害剤及びその調製方法、並びにその医薬分野での使用
JP2016505028A (ja) 3置換ピラゾール及びdlk阻害剤としての使用
US11149035B2 (en) Chemical compounds as H—PGDS inhibitors
JP2017534663A (ja) サーチュイン調節因子としての置換架橋尿素類似体
US10906905B2 (en) Five-membered heteroaryl ring bridged ring derivative, preparation method therefor and medical use thereof
KR102656524B1 (ko) 연골형성을 유도하기 위한 화합물 및 조성물
HK40112804A (en) Compounds and compositions for inducing chondrogenesis
HK1231467B (en) Compounds and compositions for inducing chondrogenesis

Legal Events

Date Code Title Description
MM4A Lapse of a eurasian patent due to non-payment of renewal fees within the time limit in the following designated state(s)

Designated state(s): AZ KG TJ TM