EA201490897A1 - Новые бензопирановые соединения, композиции и их применение - Google Patents

Новые бензопирановые соединения, композиции и их применение

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Publication number
EA201490897A1
EA201490897A1 EA201490897A EA201490897A EA201490897A1 EA 201490897 A1 EA201490897 A1 EA 201490897A1 EA 201490897 A EA201490897 A EA 201490897A EA 201490897 A EA201490897 A EA 201490897A EA 201490897 A1 EA201490897 A1 EA 201490897A1
Authority
EA
Eurasian Patent Office
Prior art keywords
compounds
compositions
application
chromen
methylpyrrolidin
Prior art date
Application number
EA201490897A
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English (en)
Inventor
Питер Дж. Кушнер
Дэвид К. Майлс
Сирус Л. Хармон
Лесли Кэрол Ходжс Гэллэгер
Original Assignee
Олема Фармасьютикалс, 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.)
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Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=48613277&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=EA201490897(A1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Олема Фармасьютикалс, Инк. filed Critical Олема Фармасьютикалс, Инк.
Publication of EA201490897A1 publication Critical patent/EA201490897A1/ru

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    • 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
    • C07D405/02—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 two hetero rings
    • C07D405/12—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 two hetero rings linked by a chain containing hetero atoms as chain links
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
    • A61K31/4025—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil not condensed and containing further heterocyclic rings, e.g. cromakalim
    • 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
    • A61K31/56—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
    • A61K31/565—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids not substituted in position 17 beta by a carbon atom, e.g. estrane, estradiol
    • 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
    • A61K31/66—Phosphorus compounds
    • A61K31/675—Phosphorus compounds having nitrogen as a ring hetero atom, e.g. pyridoxal phosphate
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • A61P15/02—Drugs for genital or sexual disorders; Contraceptives for disorders of the vagina
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • A61P15/12—Drugs for genital or sexual disorders; Contraceptives for climacteric disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • A61P19/10—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease for osteoporosis
    • 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
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00—Drugs for disorders of the endocrine system
    • A61P5/24—Drugs for disorders of the endocrine system of the sex hormones
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic System
    • C07F9/02—Phosphorus compounds
    • C07F9/06—Phosphorus compounds without P—C bonds
    • C07F9/08—Esters of oxyacids of phosphorus
    • C07F9/09—Esters of phosphoric acids
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic System
    • C07F9/02—Phosphorus compounds
    • C07F9/547—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
    • C07F9/6558—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing at least two different or differently substituted hetero rings neither condensed among themselves nor condensed with a common carbocyclic ring or ring system
    • C07F9/65586—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing at least two different or differently substituted hetero rings neither condensed among themselves nor condensed with a common carbocyclic ring or ring system at least one of the hetero rings does not contain nitrogen as ring hetero atom
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic System
    • C07F9/02—Phosphorus compounds
    • C07F9/547—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
    • C07F9/6561—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing systems of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring or ring system, with or without other non-condensed hetero rings

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Epidemiology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Endocrinology (AREA)
  • Biochemistry (AREA)
  • Molecular Biology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Reproductive Health (AREA)
  • Rheumatology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Pulmonology (AREA)
  • Gynecology & Obstetrics (AREA)
  • Diabetes (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)

Abstract

Предложены бензопирановые соединения с сильной антиэстрогенной активностью и, по существу, без эстрогенной активности, которые представляют собой ОР-1038, который является 3-(4-гидроксифенил)-4-метил-2-(4-{2-[(3R)-3-метилпирролидин-1-ил]этокси}фенил)-2Н-хромен-7-олом, и ОР-1074, который является (2S)-3-(4-гидроксифенил)-4-метил-2-(4-{2-[(3R)-3-метилпирролидин-1-ил]этокси}фенил)-2Н-хромен-7-олом. ОР-1074 является чистым антиэстрогеном при тестировании в режиме оценки действия в качестве агониста и полным антиэстрогеном при тестировании в режиме оценки действия в качестве антагониста. Эти соединения полезны для лечения или предупреждения различных состояний, которые модулируются через рецептор эстрогенов, у млекопитающих, включая людей.
EA201490897A 2011-12-16 2012-12-17 Новые бензопирановые соединения, композиции и их применение EA201490897A1 (ru)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US201161576890P 2011-12-16 2011-12-16
PCT/US2012/070168 WO2013090921A1 (en) 2011-12-16 2012-12-17 Novel benzopyran compounds, compositions and uses thereof

Publications (1)

Publication Number Publication Date
EA201490897A1 true EA201490897A1 (ru) 2015-03-31

Family

ID=48613277

Family Applications (1)

Application Number Title Priority Date Filing Date
EA201490897A EA201490897A1 (ru) 2011-12-16 2012-12-17 Новые бензопирановые соединения, композиции и их применение

Country Status (27)

Country Link
US (2) US9018244B2 (ru)
EP (1) EP2791128A4 (ru)
JP (1) JP2015505856A (ru)
KR (1) KR20140103335A (ru)
CN (1) CN104169266A (ru)
AP (1) AP2014007657A0 (ru)
AU (1) AU2012353660A1 (ru)
BR (1) BR112014014767A2 (ru)
CA (1) CA2857061A1 (ru)
CL (1) CL2014001533A1 (ru)
CR (1) CR20140259A (ru)
CU (1) CU20140066A7 (ru)
DO (1) DOP2014000135A (ru)
EA (1) EA201490897A1 (ru)
EC (1) ECSP14009619A (ru)
HK (1) HK1199246A1 (ru)
IL (1) IL233118A0 (ru)
MA (1) MA35722B1 (ru)
MD (1) MD20140054A2 (ru)
MX (1) MX2014007198A (ru)
NI (1) NI201400057A (ru)
PE (1) PE20150099A1 (ru)
PH (1) PH12014501237A1 (ru)
SG (1) SG11201402564QA (ru)
TN (1) TN2014000243A1 (ru)
WO (1) WO2013090921A1 (ru)
ZA (1) ZA201404733B (ru)

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AP2014007657A0 (en) 2014-05-31
ECSP14009619A (es) 2015-09-30
US20150197506A1 (en) 2015-07-16
HK1199246A1 (en) 2015-06-26
TN2014000243A1 (fr) 2015-09-30
US9018244B2 (en) 2015-04-28
MA35722B1 (fr) 2014-12-01
EP2791128A4 (en) 2015-04-22
SG11201402564QA (en) 2014-09-26
MD20140054A2 (ru) 2014-10-31
CN104169266A (zh) 2014-11-26
JP2015505856A (ja) 2015-02-26
CU20140066A7 (es) 2014-10-02
EP2791128A1 (en) 2014-10-22
DOP2014000135A (es) 2014-08-31
AU2012353660A1 (en) 2014-06-12
NI201400057A (es) 2014-10-01
US20130178445A1 (en) 2013-07-11
BR112014014767A2 (pt) 2017-06-13
CA2857061A1 (en) 2013-06-20
CR20140259A (es) 2014-08-21
IL233118A0 (en) 2014-08-03
CL2014001533A1 (es) 2014-10-17
MX2014007198A (es) 2014-10-13
WO2013090921A1 (en) 2013-06-20
PH12014501237A1 (en) 2014-09-08
KR20140103335A (ko) 2014-08-26
ZA201404733B (en) 2016-04-28
PE20150099A1 (es) 2015-01-30

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