EA201000971A1 - Модуляторы каннабиноидного рецептора - Google Patents

Модуляторы каннабиноидного рецептора

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Publication number
EA201000971A1
EA201000971A1 EA201000971A EA201000971A EA201000971A1 EA 201000971 A1 EA201000971 A1 EA 201000971A1 EA 201000971 A EA201000971 A EA 201000971A EA 201000971 A EA201000971 A EA 201000971A EA 201000971 A1 EA201000971 A1 EA 201000971A1
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EA
Eurasian Patent Office
Prior art keywords
alkyl
hydrogen
formula
radical
ring
Prior art date
Application number
EA201000971A
Other languages
English (en)
Other versions
EA018900B1 (ru
Inventor
Жан-Мари Ресевёр
Эмели Бьюрлинг
Энтони Мюррей
Томас Хёгберг
Петер Одаль Нильсен
Жан-Мишель Линже
Пиа Карина Ноэрегор
Дортэ Альмхольт
Original Assignee
7ТиЭм ФАРМА А/С
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
Priority claimed from GB0724096A external-priority patent/GB0724096D0/en
Priority claimed from GB0813350A external-priority patent/GB0813350D0/en
Application filed by 7ТиЭм ФАРМА А/С filed Critical 7ТиЭм ФАРМА А/С
Publication of EA201000971A1 publication Critical patent/EA201000971A1/ru
Publication of EA018900B1 publication Critical patent/EA018900B1/ru

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/06—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
    • 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
    • A61P1/14—Prodigestives, e.g. acids, enzymes, appetite stimulants, antidyspeptics, tonics, antiflatulents
    • 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
    • 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
    • A61P15/10—Drugs for genital or sexual disorders; Contraceptives for impotence
    • 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
    • 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
    • A61P25/02—Drugs for disorders of the nervous system for peripheral neuropathies
    • 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
    • A61P25/18—Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
    • 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
    • A61P25/30—Drugs for disorders of the nervous system for treating abuse or dependence
    • 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
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D231/00—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
    • C07D231/02—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings
    • C07D231/10—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D231/14—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond

Landscapes

  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Diabetes (AREA)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Endocrinology (AREA)
  • Obesity (AREA)
  • Hematology (AREA)
  • Reproductive Health (AREA)
  • Psychiatry (AREA)
  • Cardiology (AREA)
  • Addiction (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Child & Adolescent Psychology (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Nutrition Science (AREA)
  • Emergency Medicine (AREA)
  • Gynecology & Obstetrics (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)

Abstract

Соединения формулы (I) являются модуляторами каннабиноидного рецептора СВ1, применяемого наряду с прочим для лечения ожирениягде Х означает связь или двухвалентный радикал, выбранный из -C(R)(R)-*, -C(R)(R)-O-*, -C(R)(R)CH-*, -C(R)(R)CH-O-*, -CHC(R)(R))-*, -CHC(R)(R)-O-* и -CH-O-C(R)(R)-*, где связь, обозначенная звёздочкой, присоединена к пиразольному кольцу; Z обозначает карбоксильный изостерный радикал, выбранный из определённой группы; Rобозначает водород, (C-С)алкил или (C-С)фторалкил; Rобозначает радикал формулы -(Alk)-(Q)-(L)-Q, где р, r, s, Alk, L, Qи Qимеют указанные значения; или Rи R, взятые вместе с атомом азота, к которому они присоединены, образуют циклическое аминное кольцо, содержащее в кольце 4-7 атомов, которое может быть замещено радикалом формулы -(L)-Q, где s, L и Qопределены выше, или заместителем, выбранным из гидрокси, метокси, -NH- или моно- или ди-(С-С)алкиламино;R, R, Rи Rкаждый независимо выбраны из водорода, -F, -Cl, -Br -CN, (C-С)алкила, (C-С) фторалкила, циклопропила и -OR; Rобозначает водород, (C-С)алкил, гидроксил или NHи Rобозначает водород или (C-С)алкил; или Rи R, взятые вместе с атомом углерода, к которому они присоединены, образуют (С-С)циклоалкильное кольцо.
EA201000971A 2007-12-10 2008-12-08 Соединения, модулирующие активность каннабиноидного рецептора св1, композиции на их основе и их применение EA018900B1 (ru)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
GB0724096A GB0724096D0 (en) 2007-12-10 2007-12-10 Cannabinoid receptor modulators
GB0813350A GB0813350D0 (en) 2008-07-21 2008-07-21 Cannabinoid receptor modulators
PCT/GB2008/004051 WO2009074782A1 (en) 2007-12-10 2008-12-08 Cannabinoid receptor modulators

Publications (2)

Publication Number Publication Date
EA201000971A1 true EA201000971A1 (ru) 2011-02-28
EA018900B1 EA018900B1 (ru) 2013-11-29

Family

ID=40344724

Family Applications (1)

Application Number Title Priority Date Filing Date
EA201000971A EA018900B1 (ru) 2007-12-10 2008-12-08 Соединения, модулирующие активность каннабиноидного рецептора св1, композиции на их основе и их применение

Country Status (14)

Country Link
US (1) US8173680B2 (ru)
EP (1) EP2231615A1 (ru)
JP (1) JP2011506410A (ru)
KR (1) KR20100091255A (ru)
CN (1) CN101896465A (ru)
AU (1) AU2008334489A1 (ru)
BR (1) BRPI0822061A2 (ru)
CA (1) CA2708706A1 (ru)
EA (1) EA018900B1 (ru)
IL (1) IL205980A0 (ru)
MX (1) MX2010006109A (ru)
NZ (1) NZ585704A (ru)
WO (1) WO2009074782A1 (ru)
ZA (1) ZA201004828B (ru)

Families Citing this family (9)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
TWI532725B (zh) * 2010-01-26 2016-05-11 賽諾菲阿凡提斯公司 經氧取代之３－雜芳醯基胺基－丙酸衍生物及其作為藥物之用途
BR112013013490B1 (pt) * 2011-09-30 2019-10-22 National Health Research Institutes compostos e composição farmacêutica
EP2822931B1 (en) 2012-03-09 2017-05-03 Inception 2, Inc. Triazolone compounds and uses thereof
IN2015DN03733A (ru) 2012-11-13 2015-09-18 Us Health
US11155521B2 (en) * 2012-11-13 2021-10-26 The United States Of America As Represented By The Secretary, Department Of Health And Human Services Cannabinoid receptor mediating compounds
MX2015007433A (es) 2012-12-20 2015-12-07 Inception 2 Inc Compuestos de triazolona y usos de los mismos.
EA201690230A1 (ru) 2013-09-06 2016-07-29 Инсепшн 2, Инк. Соединения триазолона и их применения
CA2948349C (en) 2014-05-09 2023-03-28 The United States Of America, As Represented By The Secretary, Department Of Health And Human Services Pyrazole derivatives and their use as cannabinoid receptor mediators
US11091447B2 (en) 2020-01-03 2021-08-17 Berg Llc UBE2K modulators and methods for their use

Family Cites Families (10)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
FR2741621B1 (fr) * 1995-11-23 1998-02-13 Sanofi Sa Nouveaux derives de pyrazole, procede pour leur preparation et compositions pharmaceutiques en contenant
FR2856683A1 (fr) 2003-06-25 2004-12-31 Sanofi Synthelabo Derives de 4-cyanopyrazole-3-carboxamide, leur preparation et leur application en therapeutique
CA2585175A1 (en) * 2004-10-25 2006-05-04 Solvay Pharmaceuticals Gmbh Pharmaceutical compositions comprising cb1 cannabinoid receptor antagonists and potassium channel openers for the treatment of diabetes mellitus type i, obesity and related conditions
EP1831177A1 (en) * 2004-12-23 2007-09-12 AstraZeneca AB Therapeutic agents
EP1928859A1 (en) * 2005-06-17 2008-06-11 Carex SA Pyrazole derivates as cannabinoid receptor modulators
JP5069894B2 (ja) * 2005-10-21 2012-11-07 田辺三菱製薬株式会社 ピラゾール化合物
EP1993560B1 (en) * 2006-03-10 2011-12-28 Jenrin Discovery Cannabinoid receptor antagonists/inverse agonists useful for treating obesity
AU2007267097A1 (en) * 2006-05-31 2007-12-06 Solvay Pharmaceuticals B.V. Sulphur containing pyrazole derivatives as selective cannabinoid CB1 receptor antagonists
GB0622569D0 (en) 2006-11-11 2006-12-20 7Tm Pharma As Cannabinoid receptor modulators
MX2009006214A (es) 2006-12-18 2009-06-22 7Tm Pharma As Moduladores del receptor cb1.

Also Published As

Publication number Publication date
US20100292273A1 (en) 2010-11-18
CA2708706A1 (en) 2009-06-18
WO2009074782A1 (en) 2009-06-18
ZA201004828B (en) 2011-03-30
AU2008334489A1 (en) 2009-06-18
BRPI0822061A2 (pt) 2015-06-23
US8173680B2 (en) 2012-05-08
CN101896465A (zh) 2010-11-24
IL205980A0 (en) 2010-11-30
NZ585704A (en) 2012-08-31
KR20100091255A (ko) 2010-08-18
MX2010006109A (es) 2010-09-10
EA018900B1 (ru) 2013-11-29
JP2011506410A (ja) 2011-03-03
EP2231615A1 (en) 2010-09-29

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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): AM AZ BY KZ KG MD TJ TM RU