PE20090549A1 - Derivados de imidazolidinona con actividad sobre lxr-alfa y lxr-beta - Google Patents

Derivados de imidazolidinona con actividad sobre lxr-alfa y lxr-beta

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Publication number
PE20090549A1
PE20090549A1 PE2008000551A PE2008000551A PE20090549A1 PE 20090549 A1 PE20090549 A1 PE 20090549A1 PE 2008000551 A PE2008000551 A PE 2008000551A PE 2008000551 A PE2008000551 A PE 2008000551A PE 20090549 A1 PE20090549 A1 PE 20090549A1
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PE
Peru
Prior art keywords
phenyl
lxr
alkyl
beta
alpha
Prior art date
Application number
PE2008000551A
Other languages
English (en)
Inventor
Henrietta Dehmlow
Bernd Kuhn
Stephan Roever
Tanja Schulz-Gasch
Matthew Wright
Ulrike Obst Sander
Original Assignee
Hoffmann La Roche
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 Hoffmann La Roche filed Critical Hoffmann La Roche
Publication of PE20090549A1 publication Critical patent/PE20090549A1/es

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    • 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
    • C07D403/06—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 linked by a carbon chain containing only aliphatic carbon atoms
    • 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
    • A61K31/495—Heterocyclic 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
    • A61K31/496—Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
    • 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
    • A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
    • 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
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/18—Drugs for disorders of the alimentary tract or the digestive system for pancreatic disorders, e.g. pancreatic enzymes
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/06—Antipsoriatics
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • 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
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/04—Antibacterial agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • A61P31/14—Antivirals for RNA viruses
    • A61P31/18—Antivirals for RNA viruses for HIV
    • 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
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    • 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
    • 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
    • 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
    • C07D403/14—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 three or more hetero rings
    • 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
    • C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D495/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
    • C07D495/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D495/04—Ortho-condensed systems

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Diabetes (AREA)
  • Oncology (AREA)
  • Communicable Diseases (AREA)
  • Obesity (AREA)
  • Hematology (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Virology (AREA)
  • Dermatology (AREA)
  • Biomedical Technology (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • Urology & Nephrology (AREA)
  • Rheumatology (AREA)
  • Pain & Pain Management (AREA)
  • Gastroenterology & Hepatology (AREA)
  • AIDS & HIV (AREA)
  • Psychiatry (AREA)
  • Molecular Biology (AREA)
  • Ophthalmology & Optometry (AREA)
  • Hospice & Palliative Care (AREA)
  • Vascular Medicine (AREA)
  • Cardiology (AREA)
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  • Emergency Medicine (AREA)
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Abstract

REFERIDA UN COMPUESTO DERIVADO DE IMIDAZOLIDINONA DE FORMULA (I), DONDE X ES N O CH; R1 ES ALQUILO C1-C7, FLUOR-ALQUILO C1-C7, CICLOALQUILO C3-C10, ENTRE OTROS; R2 ES ALQUILO C1-C7, HALOGENO-ALQUILO C1-C7, CICLOALQUILO C3-C10, ENTRE OTROS; R3 ES ARILO TAL COMO FENILO O NAFTILO, O HETEROARILO AROMATICO MONOCICLICO DE 5 O 6 MIEMBROS O BICICLICO DE 9 A 10 MIEMBROS, QUE CONTIENEN DE 1 A 3 ATOMOS DE N, O O S, ENTRE OTROS; R4, R5, R6, R7, R8, R9, R10 Y R11 SON H O ALQUILO C1-C7. SON COMPUESTOS PREFERIDOS: (RS)-4-[4-(2,5-DIMETIL-FENIL)-PIPERAZINA-1-CARBONIL]-1-(3-METOXI-BENCENOSULFONIL)-3-FENIL-IMIDAZOLIDIN-2-ONA, (RS)-1-BENCENOSULFONIL-4-[4-(2,5-DIMETIL-FENIL)-PIPERAZINA-1-CARBONIL]-3-FENIL-IMIDAZOLIDIN-2-ONA, (RS)-1-(3-METOXI-BENCENOSULFONIL)-3-FENIL-4-[4-(3-TRIFLUORMETIL-FENIL)-PIPERAZINA-1-CARBONIL]-IMIDAZOLIDIN-2-ONA, ENTRE OTROS. TAMBIEN ESTA REFERIDA A UNA COMPOSICION FARMACEUTICA. DICHOS COMPUESTOS TIENEN ACTIVIDAD SOBRE LOS RECEPTORES X DEL HIGADO, PARTICULARMENTE, LXR-ALFA Y LXR-BETA Y SON UTILES EN EL TRATAMIENTO DE DISLIPIDEMIAS
PE2008000551A 2007-03-30 2008-03-27 Derivados de imidazolidinona con actividad sobre lxr-alfa y lxr-beta PE20090549A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
EP07105376 2007-03-30

Publications (1)

Publication Number Publication Date
PE20090549A1 true PE20090549A1 (es) 2009-05-09

Family

ID=39661434

Family Applications (1)

Application Number Title Priority Date Filing Date
PE2008000551A PE20090549A1 (es) 2007-03-30 2008-03-27 Derivados de imidazolidinona con actividad sobre lxr-alfa y lxr-beta

Country Status (22)

Country Link
US (1) US7625902B2 (es)
EP (1) EP2142533B1 (es)
JP (1) JP5165748B2 (es)
KR (1) KR101171433B1 (es)
CN (1) CN101641348B (es)
AR (1) AR065863A1 (es)
AT (1) ATE533761T1 (es)
AU (1) AU2008234017B2 (es)
BR (1) BRPI0809680A2 (es)
CA (1) CA2681809C (es)
CL (1) CL2008000875A1 (es)
DK (1) DK2142533T3 (es)
ES (1) ES2375586T3 (es)
IL (1) IL200868A0 (es)
MX (1) MX2009010567A (es)
PE (1) PE20090549A1 (es)
PL (1) PL2142533T3 (es)
PT (1) PT2142533E (es)
RU (1) RU2437882C2 (es)
TW (1) TWI348908B (es)
WO (1) WO2008119657A1 (es)
ZA (1) ZA200906467B (es)

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CN101778831B (zh) * 2007-08-13 2014-08-20 霍夫曼-拉罗奇有限公司 哌嗪酰胺衍生物
WO2009097995A1 (de) * 2008-02-07 2009-08-13 Sanofi-Aventis Neue phenyl-substituierte imidazolidine, verfahren zu deren herstellung, diese verbindungen enthaltende arzneimittel und deren verwendung
US8933024B2 (en) 2010-06-18 2015-01-13 Sanofi Azolopyridin-3-one derivatives as inhibitors of lipases and phospholipases
BR112013005425A2 (pt) 2010-09-07 2018-05-02 Snu R&Db Foundation compostos sesterterpenos e suas utilizações
HUE045701T2 (hu) 2013-03-13 2020-01-28 Forma Therapeutics Inc 2-Hidroxi-1-{4-[(4-fenilfenil)karbonil]piperazin-1-il}etán-1-on származékok és rokon vegyületek mint zsírsav szintáz (FASN) inhibitorok, rák kezelésére
EP3373935B1 (en) * 2015-11-12 2021-09-01 Merck Sharp & Dohme Corp. Cyanopyridine derivatives as liver x receptor beta agonists, compositions, and their use
EA039859B1 (ru) 2016-02-03 2022-03-21 Эмджен Рисерч (Мюник) Гмбх Биспецифические конструкты антител, связывающие egfrviii и cd3
WO2019023448A1 (en) * 2017-07-26 2019-01-31 Emory University INHIBITORS OF NADPH OXIDASE AND THEIR USE
TWI748194B (zh) 2018-06-28 2021-12-01 德商菲尼克斯 Ｆｘｒ有限責任公司 含有雙環核心部分之新穎lxr調節劑
TWI767148B (zh) 2018-10-10 2022-06-11 美商弗瑪治療公司 抑制脂肪酸合成酶(fasn)
CN113382633A (zh) 2018-10-29 2021-09-10 福马治疗股份有限公司 (4-(2-氟-4-(1-甲基-1H-苯并[d]咪唑-5-基)苯甲酰基)哌嗪-1-基)(1-羟基环丙基)甲酮的固体形式
US20230039836A1 (en) * 2020-01-10 2023-02-09 Uniwersytet Jagiellonski Aromatic sulphonamides derivatives that inhibits pdi a3, their synthesis and use
WO2021141507A1 (en) * 2020-01-10 2021-07-15 Uniwersytet Jagielloński Aromatic sulphonamides derivatives that inhibits pdi a3, their synthesis and use

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EP0966462B1 (en) * 1997-02-13 2003-06-11 AstraZeneca AB Heterocyclic compounds useful as oxido-squalene cyclase inhibitors
US6316503B1 (en) * 1999-03-15 2001-11-13 Tularik Inc. LXR modulators
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US20040072868A1 (en) * 2000-09-18 2004-04-15 Collins Jon Loren Substitued aminopropoxyaryl derivatives useful as agonists for lxr
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Also Published As

Publication number Publication date
ES2375586T3 (es) 2012-03-02
AU2008234017A1 (en) 2008-10-09
CN101641348A (zh) 2010-02-03
CA2681809C (en) 2012-06-05
AR065863A1 (es) 2009-07-08
ATE533761T1 (de) 2011-12-15
KR101171433B1 (ko) 2012-08-06
CL2008000875A1 (es) 2008-10-03
PT2142533E (pt) 2012-01-19
KR20090130090A (ko) 2009-12-17
AU2008234017B2 (en) 2011-09-22
DK2142533T3 (da) 2011-12-12
RU2009139915A (ru) 2011-05-10
JP2010523514A (ja) 2010-07-15
JP5165748B2 (ja) 2013-03-21
ZA200906467B (en) 2010-05-26
CN101641348B (zh) 2014-09-10
TW200848046A (en) 2008-12-16
TWI348908B (en) 2011-09-21
BRPI0809680A2 (pt) 2014-10-07
EP2142533B1 (en) 2011-11-16
WO2008119657A1 (en) 2008-10-09
IL200868A0 (en) 2010-05-17
CA2681809A1 (en) 2008-10-09
MX2009010567A (es) 2009-10-22
US7625902B2 (en) 2009-12-01
EP2142533A1 (en) 2010-01-13
RU2437882C2 (ru) 2011-12-27
US20080242677A1 (en) 2008-10-02
PL2142533T3 (pl) 2012-04-30

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