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PE20060503A1 - Prodroga de benzoxazoles substituidos como agentes estrogenicos - Google Patents

Prodroga de benzoxazoles substituidos como agentes estrogenicos

Info

Publication number
PE20060503A1
PE20060503A1 PE2005000978A PE2005000978A PE20060503A1 PE 20060503 A1 PE20060503 A1 PE 20060503A1 PE 2005000978 A PE2005000978 A PE 2005000978A PE 2005000978 A PE2005000978 A PE 2005000978A PE 20060503 A1 PE20060503 A1 PE 20060503A1
Authority
PE
Peru
Prior art keywords
benzoxazole
fluoro
halogen
vinyl
alkyl
Prior art date
Application number
PE2005000978A
Other languages
English (en)
Inventor
Sayed Elmarakby
Ping Cai
Mark Ruppen
Rasmy Talaat
Appavu Chandrasekaran
Original Assignee
Wyeth Corp
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 Wyeth Corp filed Critical Wyeth Corp
Publication of PE20060503A1 publication Critical patent/PE20060503A1/es

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D263/00Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings
    • C07D263/52Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings condensed with carbocyclic rings or ring systems
    • C07D263/54Benzoxazoles; Hydrogenated benzoxazoles
    • C07D263/56Benzoxazoles; Hydrogenated benzoxazoles with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached in position 2
    • C07D263/57Aryl or substituted aryl radicals
    • 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
    • A61K31/42Oxazoles
    • A61K31/423Oxazoles condensed with carbocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04Drugs 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • A61P11/06Antiasthmatics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00Drugs for disorders of the urinary system
    • A61P13/08Drugs for disorders of the urinary system of the prostate
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00Drugs for disorders of the urinary system
    • A61P13/10Drugs for disorders of the urinary system of the bladder
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00Drugs for genital or sexual disorders; Contraceptives
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00Drugs for genital or sexual disorders; Contraceptives
    • A61P15/18Feminine contraceptives
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • A61P17/06Antipsoriatics
    • 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
    • A61P25/00Drugs for disorders of the nervous system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/22Anxiolytics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/28Drugs 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/06Antihyperlipidemics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/08Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P39/00General protective or antinoxious agents
    • A61P39/06Free radical scavengers or antioxidants
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00Drugs for disorders of the endocrine system
    • A61P5/24Drugs for disorders of the endocrine system of the sex hormones
    • A61P5/30Oestrogens
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/10Drugs 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/12Antihypertensives
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D413/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02Heterocyclic 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
    • C07D413/04Heterocyclic 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 directly linked by a ring-member-to-ring-member bond
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D417/00Heterocyclic 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
    • C07D417/02Heterocyclic 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 two hetero rings
    • C07D417/04Heterocyclic 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 two hetero rings directly linked by a ring-member-to-ring-member bond

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Public Health (AREA)
  • Animal Behavior & Ethology (AREA)
  • Veterinary Medicine (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Diabetes (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Endocrinology (AREA)
  • Urology & Nephrology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Pulmonology (AREA)
  • Cardiology (AREA)
  • Dermatology (AREA)
  • Rheumatology (AREA)
  • Reproductive Health (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Immunology (AREA)
  • Gynecology & Obstetrics (AREA)
  • Hospice & Palliative Care (AREA)
  • Psychiatry (AREA)
  • Vascular Medicine (AREA)
  • Biochemistry (AREA)
  • Toxicology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Pain & Pain Management (AREA)
  • Emergency Medicine (AREA)

Abstract

SE REFIERE A UN COMPUESTO DE FORMULA I, DONDE Q1 Y Q2 SON CADA UNO H, UN RESIDUO DE AZUCAR, S(O)t-OH; t ES 0-2; R1 ES H, HIDROXILO, HALOGENO, ENTRE OTROS; R2 Y R2a SON CADA UNO H, HIDROXILO, HALOGENO, ALQUILO C1-C6, ALCOXI C1-C4, ALQUINILO C2-C7, ENTRE OTROS; R3 Y R3a SON CADA UNO H, ALQUILO C1-C3, ALQUENILO C2-C7, HALOGENO, ALCOXI C1-C4, ENTRE OTROS; X ES O, S, NH, ENTRE OTROS. SON COMPUESTOS PREFERIDOS: 2-(3'-FLUORO-4'-GLUCURONIDO FENIL)-7-VINIL-1,3-BENZOXAZOL-5-GLUCURONIDO; 2-(3'-FLUORO-4'-SULFATO FENIL)-7-VINIL-1,3-BENZOXAZOL-5-SULFATO; 2-(2'-FLUORO-4'-HIDROXIFENIL)-7-VINIL-1,3-BENZOXAZOL-5-GLUCURONIDO; ENTRE OTROS. SE REFIERE TAMBIEN A UNA COMPOSICION FARMACEUTICA. DICHOS COMPUESTOS SON MODULADORES DEL RECEPTOR DE ESTROGENOS UTILES EN DESORDENES METABOLICOS COMO METABOLISMO DE LIPIDOS, APETITO, DESORDENES DE SANGRAMIENTO TALES COMO TELANGIECTASIA HEMORRAGICA HEREDITARIA, SANGRAMIENTO DEL UTERO DISFUNCIONAL, ENTRE OTROS
PE2005000978A 2004-08-26 2005-08-24 Prodroga de benzoxazoles substituidos como agentes estrogenicos PE20060503A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US60483504P 2004-08-26 2004-08-26

Publications (1)

Publication Number Publication Date
PE20060503A1 true PE20060503A1 (es) 2006-07-20

Family

ID=35750972

Family Applications (1)

Application Number Title Priority Date Filing Date
PE2005000978A PE20060503A1 (es) 2004-08-26 2005-08-24 Prodroga de benzoxazoles substituidos como agentes estrogenicos

Country Status (22)

Country Link
US (2) US20060046968A1 (es)
EP (1) EP1781628A2 (es)
JP (1) JP2008510827A (es)
KR (1) KR20070046148A (es)
CN (1) CN101044126A (es)
AR (1) AR050618A1 (es)
AU (1) AU2005280178A1 (es)
BR (1) BRPI0514628A (es)
CA (1) CA2576353A1 (es)
CL (1) CL2008000506A1 (es)
CR (1) CR8931A (es)
EC (1) ECSP077279A (es)
GT (1) GT200500228A (es)
IL (1) IL181236A0 (es)
MX (1) MX2007002251A (es)
NI (1) NI200700055A (es)
NO (1) NO20071159L (es)
PE (1) PE20060503A1 (es)
RU (1) RU2007105232A (es)
SV (1) SV2006002205A (es)
TW (1) TW200612925A (es)
WO (1) WO2006026316A2 (es)

Families Citing this family (13)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
UA83620C2 (ru) * 2001-12-05 2008-08-11 Уайт Замещенные бензоксазолы и их аналоги как эстрогенные агенты
TW200800180A (en) * 2006-03-06 2008-01-01 Wyeth Corp Liquid and semi-solid pharmaceutical formulations and processes
WO2008057309A2 (en) * 2006-11-02 2008-05-15 Merck & Co., Inc. Estrogen receptor modulators
WO2008067425A1 (en) * 2006-11-30 2008-06-05 Wyeth Process for the synthesis of monosulfated derivatives of substituted benzoxazoles
CL2007003443A1 (es) * 2006-11-30 2008-07-11 Wyeth6 3 Compuestos derivados de benzoxazoles sustituidos; procedimiento de preparacion, utiles como agentes estrogenicos.
US20090010884A1 (en) * 2007-07-06 2009-01-08 Wyeth Pharmaceutical compositions and methods of preventing, treating, or inhibiting inflammatory diseases, disorders, or conditions of the skin, and diseases, disorders, or conditions associated with collagen depletion
US20110212923A1 (en) * 2008-02-08 2011-09-01 Pfizer Inc. Phosphate Derivatives of Substituted Benzoxazoles
WO2010036908A1 (en) * 2008-09-26 2010-04-01 Eisai R & D Management Co., Ltd. Use of benzoxazole compounds in the treatment of malaria
WO2010036905A1 (en) * 2008-09-26 2010-04-01 Eisai R & D Management Co., Ltd. Benzoxazole compounds and methods of use
WO2010083220A1 (en) 2009-01-19 2010-07-22 Abbott Laboratories Benzoxazole inhibitors of poly(adp-ribose)polymerase
KR20160007029A (ko) 2014-07-10 2016-01-20 삼성전기주식회사 압전 소자 및 이를 포함하는 압전 진동 모듈
EP3263109B1 (en) 2015-02-24 2020-06-17 National University Corporation Tottori University Drug for preventing and/or treating dementia
CN117045680B (zh) * 2023-10-12 2023-12-08 北京国卫生物科技有限公司 促进肝脏再生的干细胞制剂及其制备方法

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US4418068A (en) * 1981-04-03 1983-11-29 Eli Lilly And Company Antiestrogenic and antiandrugenic benzothiophenes
AU707798B2 (en) * 1995-06-23 1999-07-22 Advanced Life Sciences Inc. Biflavanoids and derivatives thereof as antiviral agents
US5998402A (en) * 1996-04-19 1999-12-07 American Home Products Corporation 2-phenyl-1-[4-(2-aminoethoxy)-benzyl]-indoles as estrogenic agents
US5919808A (en) * 1996-10-23 1999-07-06 Zymogenetics, Inc. Compositions and methods for treating bone deficit conditions
US5948776A (en) * 1996-10-23 1999-09-07 Zymogenetic, Inc. Compositions and methods for treating bone deficit conditions
US6331562B1 (en) * 1998-12-30 2001-12-18 Signal Pharmaceuticals, Inc. Compounds and methods for modulation of estrogen receptors
WO2000062765A2 (en) * 1999-04-16 2000-10-26 Astrazeneca Ab ESTROGEN RECEPTOR-β LIGANDS
WO2002046168A1 (en) * 2000-12-07 2002-06-13 Astrazeneca Ab Therapeutic benzimidazole compounds
US7045539B2 (en) * 2000-12-22 2006-05-16 Astrazeneca Ab Therapeutic benzoxazole compounds
WO2002056969A2 (en) * 2001-01-18 2002-07-25 Acumen Manufacturing Limited 10k step exercise method and apparatus
EP1368037A2 (en) * 2001-03-16 2003-12-10 Wyeth Estrogen replacement therapy
US6559177B2 (en) * 2001-04-19 2003-05-06 Wyeth 5, 11-Dioxa-benzo[b]fluoren-10-one and 5-oxa-11-thia-benzo[b]fluoren-10-ones as estrogenic agents
UA83620C2 (ru) * 2001-12-05 2008-08-11 Уайт Замещенные бензоксазолы и их аналоги как эстрогенные агенты
SE0202429D0 (sv) * 2002-08-14 2002-08-14 Astrazeneca Ab Novel Compounds

Also Published As

Publication number Publication date
WO2006026316A2 (en) 2006-03-09
CL2008000506A1 (es) 2008-06-13
RU2007105232A (ru) 2008-10-20
ECSP077279A (es) 2007-03-29
IL181236A0 (en) 2007-07-04
US20080255057A1 (en) 2008-10-16
AR050618A1 (es) 2006-11-08
NO20071159L (no) 2007-03-26
TW200612925A (en) 2006-05-01
CR8931A (es) 2007-08-28
CA2576353A1 (en) 2006-03-09
BRPI0514628A (pt) 2008-06-17
JP2008510827A (ja) 2008-04-10
KR20070046148A (ko) 2007-05-02
US20060046968A1 (en) 2006-03-02
GT200500228A (es) 2006-06-22
NI200700055A (es) 2008-02-27
MX2007002251A (es) 2007-04-20
SV2006002205A (es) 2006-09-14
EP1781628A2 (en) 2007-05-09
CN101044126A (zh) 2007-09-26
AU2005280178A1 (en) 2006-03-09
WO2006026316A3 (en) 2006-05-26

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