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EA200602060A1 - Производные пирролидин-2-она и пиперидин-2-она, используемые в качестве ингибиторов 11-бета-гидроксистероид-дегидрогеназы - Google Patents

Производные пирролидин-2-она и пиперидин-2-она, используемые в качестве ингибиторов 11-бета-гидроксистероид-дегидрогеназы

Info

Publication number
EA200602060A1
EA200602060A1 EA200602060A EA200602060A EA200602060A1 EA 200602060 A1 EA200602060 A1 EA 200602060A1 EA 200602060 A EA200602060 A EA 200602060A EA 200602060 A EA200602060 A EA 200602060A EA 200602060 A1 EA200602060 A1 EA 200602060A1
Authority
EA
Eurasian Patent Office
Prior art keywords
6alkyl
hydroxy
halogen
optionally substituted
6alkyloxy
Prior art date
Application number
EA200602060A
Other languages
English (en)
Other versions
EA011097B1 (ru
Inventor
Либуше Яроскова
Йоаннес Теодорус Мария Линдерс
Кристоф Франсис Роберт Нестор Бюйк
Луи Йозеф Элизабет Ван Дер Векен
Владимир Димчев Димитров
Тео Теофанов Никифоров
Original Assignee
Янссен Фармацевтика Н.В.
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 Янссен Фармацевтика Н.В. filed Critical Янссен Фармацевтика Н.В.
Publication of EA200602060A1 publication Critical patent/EA200602060A1/ru
Publication of EA011097B1 publication Critical patent/EA011097B1/ru

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D211/00—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
    • C07D211/04—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D211/68—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having one double bond between ring members or between a ring member and a non-ring member
    • C07D211/72—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having one double bond between ring members or between a ring member and a non-ring member with hetero atoms or with carbon atoms having three bonds to hetero atoms, with at the most one bond to halogen, directly attached to ring carbon atoms
    • C07D211/74—Oxygen atoms
    • C07D211/76—Oxygen atoms attached in position 2 or 6
    • 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
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/02—Ophthalmic agents
    • A61P27/06—Antiglaucoma agents or miotics
    • 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
    • A61P3/04—Anorexiants; Antiobesity agents
    • 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
    • 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
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • 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
    • A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D207/00—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D207/02—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D207/18—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having one double bond between ring members or between a ring member and a non-ring member
    • C07D207/22—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having one double bond between ring members or between a ring member and a non-ring member 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
    • C07D207/24—Oxygen or sulfur atoms
    • C07D207/26—2-Pyrrolidones
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D207/00—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D207/02—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D207/18—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having one double bond between ring members or between a ring member and a non-ring member
    • C07D207/22—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having one double bond between ring members or between a ring member and a non-ring member 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
    • C07D207/24—Oxygen or sulfur atoms
    • C07D207/26—2-Pyrrolidones
    • C07D207/263—2-Pyrrolidones with only hydrogen atoms or radicals containing only hydrogen and carbon atoms directly attached to other ring carbon atoms
    • C07D207/267—2-Pyrrolidones with only hydrogen atoms or radicals containing only hydrogen and carbon atoms directly attached to other ring carbon atoms with only hydrogen atoms or radicals containing only hydrogen and carbon atoms directly attached to the ring nitrogen atom
    • 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
    • C07D405/06—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 carbon chain containing only aliphatic carbon atoms

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  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Health & Medical Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Diabetes (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Obesity (AREA)
  • Hematology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Neurology (AREA)
  • Cardiology (AREA)
  • Rheumatology (AREA)
  • Ophthalmology & Optometry (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Emergency Medicine (AREA)
  • Hospice & Palliative Care (AREA)
  • Endocrinology (AREA)
  • Psychiatry (AREA)
  • Child & Adolescent Psychology (AREA)
  • Urology & Nephrology (AREA)
  • Vascular Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Pyrrole Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Hydrogenated Pyridines (AREA)

Abstract

Описано соединение формулы (I), его N-оксидные формы, фармацевтически приемлемые аддитивные соли и стереохимически изомерные формы, где n равно 1 или 2; L представляет собой C-алкильный линкер, необязательно замещенный одним или двумя заместителями, выбранными из Салкила, Салкилокси-Салкила, гидрокси-Салкила, гидрокси, Cалкилокси или фенил-Салкила; М представляет собой прямую связь или Cалкильный линкер, необязательно замещенный одним или двумя заместителями, выбранными из гидрокси, Салкила или Салкилокси; каждый из Rи Rнезависимо представляет собой водород, галоген, циано, гидрокси, Салкил, необязательно замещенный галогеном, Салкилокси, необязательно замещенный одним или, где это возможно, двумя или тремя заместителями, выбранными из гидрокси, Arи галогена; либо Rи R, взятые вместе с фенильным кольцом, с которым они связаны, образуют нафтил или 1,3-бензодиоксолил, где указанный нафтил или 1,3-бензодиоксолил необязательно замещены галогеном; Rпредставляет собой водород, галоген, Салкил, Салкилокси, циано или гидрокси; Rпредставляет собой водород, галоген, Салкил, C-алкилокси, циано или гидрокси; Rпредставляет собой водород, Салкил или Ar-Салкил; Rпредставляет собой водород, галоген, Салкил или Салкилокси; каждый из Arи Arнезависимо представляет собой фенил или нафтил, где указанные фенил и нафтил необязательно замещены Салкилом, Салкилокси или фенилСалкилом; и где указанное соединение предназначено для использования в качестве лекарственного средства.
EA200602060A 2004-05-07 2005-04-29 Производные пирролидин-2-она и пиперидин-2-она, используемые в качестве ингибиторов 11-бета-гидроксистероид-дегидрогеназы EA011097B1 (ru)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
EP04101991 2004-05-07
PCT/EP2005/051968 WO2005108360A1 (en) 2004-05-07 2005-04-29 Pyrrolidin-2-one and piperidin-2-one derivatives as 11-beta hydroxysteroid dehydrogenase inhibitors

Publications (2)

Publication Number Publication Date
EA200602060A1 true EA200602060A1 (ru) 2007-04-27
EA011097B1 EA011097B1 (ru) 2008-12-30

Family

ID=34929074

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EA200602060A EA011097B1 (ru) 2004-05-07 2005-04-29 Производные пирролидин-2-она и пиперидин-2-она, используемые в качестве ингибиторов 11-бета-гидроксистероид-дегидрогеназы

Country Status (17)

Country Link
US (3) US9012494B2 (ru)
EP (1) EP1747199B1 (ru)
JP (1) JP5014983B2 (ru)
KR (1) KR101192861B1 (ru)
CN (1) CN101001836B (ru)
AR (1) AR048778A1 (ru)
AU (1) AU2005240784C1 (ru)
CA (1) CA2565630C (ru)
EA (1) EA011097B1 (ru)
ES (1) ES2525319T3 (ru)
IL (1) IL179065A (ru)
MX (1) MXPA06012932A (ru)
MY (1) MY161872A (ru)
NO (1) NO20065619L (ru)
NZ (1) NZ551077A (ru)
TW (1) TWI396534B (ru)
WO (1) WO2005108360A1 (ru)

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CA2565630A1 (en) 2005-11-17
US20160168094A1 (en) 2016-06-16
WO2005108360A1 (en) 2005-11-17
US20150183735A1 (en) 2015-07-02
KR20070011528A (ko) 2007-01-24
EP1747199A1 (en) 2007-01-31
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AU2005240784C1 (en) 2011-12-22
US9776965B2 (en) 2017-10-03
JP5014983B2 (ja) 2012-08-29
IL179065A (en) 2012-10-31
AR048778A1 (es) 2006-05-24
NO20065619L (no) 2006-12-06
AU2005240784A1 (en) 2005-11-17
KR101192861B1 (ko) 2012-10-19
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TWI396534B (zh) 2013-05-21
CA2565630C (en) 2013-05-28
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US9012494B2 (en) 2015-04-21
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US20080139625A1 (en) 2008-06-12
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