AR050618A1 - Conjugados de acido glucuronico de benzoxazoles substituidos como agentes estrogenicos y composiciones farmaceuticas que los contienen. - Google Patents

Conjugados de acido glucuronico de benzoxazoles substituidos como agentes estrogenicos y composiciones farmaceuticas que los contienen.

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Publication number
AR050618A1
AR050618A1 ARP050103597A ARP050103597A AR050618A1 AR 050618 A1 AR050618 A1 AR 050618A1 AR P050103597 A ARP050103597 A AR P050103597A AR P050103597 A ARP050103597 A AR P050103597A AR 050618 A1 AR050618 A1 AR 050618A1
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AR
Argentina
Prior art keywords
alkyl
trifluoroalkoxy
trifluoroalkyl
halogen
alkenyl
Prior art date
Application number
ARP050103597A
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English (en)
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Wyeth Corp
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Publication of AR050618A1 publication Critical patent/AR050618A1/es

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    • 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

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

Abstract

Se proprociona moduladores del receptor de estrogenos y composiciones farmacéuticas que los contienen. Reivindicacion 1: Un compuesto de la formula (1), caracterizado porque tiene la siguiente estructura: en donde: Q1 y Q2 son independientemente H, un residuo de azucar o S(O)t-OH, con la condicion de que Q1 y Q2 no sean ambos H; t es 0, 1 o 2; R1 es H, hidroxilo, halogeno, alquilo C1-6, trifluoroalquilo C1-6, cicloalquilo C3-8, alcoxi C1-6, trifluoroalcoxi C1-6, tioalquilo C1-6, sulfoxoalquilo C1-8, sulfonoalquilo C1-6, arilo C6-10, un anillo heterocíclico de 5 u 8 miembros que tiene 1 a 4 heteroátomos seleccioandos a partir de O, N o S, -NO2, -NR5R6, -N(R5)COR6, -CN, -CHFCN, -CF2CN, alquinilo C2-7, o alquenilo C2-7, en donde las porciones alquilo o alquenilo son opcionalmente substituidas con hidroxilo, -CN, halogeno, trifluoroalquilo, trifluoroalcoxi, -COR5, -CO2R5, -NO2, CONR5R6, NR5R6 o N(R5)COR6; R2 y R2a son cada uno, independientemente, h, hidroxilo, halogeno, alquilo C1-6, alcoxi C1-4, alquenilo C2-7, alquinilo C2-7, trifluoroalquilo C1-6, o trifluoroalcoxi C1-6; en donde las porciones alquilo, alquenilo, o alquinilo son opcionalmente substituidas con hidroxilo, -CN, halogeno, trifluoroalquilo, trifluoroalcoxi, - COR5, -CO2R5, -NO2, CONR5R6, NR5R6 o N(R5)COR6; R3 y R3a son cada uno, independientemente, H, alquilo C1-3, alquenilo C2-7, alquinilo C2-7, halogeno, alcoxi C1-4, trifluoroalquilo C1-6, o trifluoroalcoxi C1-6; en donde las porciones alquilo, alquenilo, o alquinilo son opcionalmente substituidas con hidroxilo, -CN, halogeno, trifluoroalquilo, trifluoroalcoxi, -COR5, -CO2R5, -NO2, CONR5R6, NR5R6 o N(R5)COR6; R5, R6 son cada uno, independientemente H, alquilo C1-6, arilo C6-10, X es O, S, o NR7; R7 es H, alquilo C1-6, arilo C6-10, -COR5, -CO2R5, o -SO2R5; o una sal farmacéuticamente aceptable de los mismos.
ARP050103597A 2004-08-26 2005-08-26 Conjugados de acido glucuronico de benzoxazoles substituidos como agentes estrogenicos y composiciones farmaceuticas que los contienen. AR050618A1 (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
AR050618A1 true AR050618A1 (es) 2006-11-08

Family

ID=35750972

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Application Number Title Priority Date Filing Date
ARP050103597A AR050618A1 (es) 2004-08-26 2005-08-26 Conjugados de acido glucuronico de benzoxazoles substituidos como agentes estrogenicos y composiciones farmaceuticas que los contienen.

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)

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* 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
AR064029A1 (es) * 2006-11-30 2009-03-04 Wyeth Corp Proceso para la sintesis de derivados monosulfatados de benzoxazoles sustituidos
AR064030A1 (es) * 2006-11-30 2009-03-04 Wyeth Corp Proceso para la sintesis de derivados monosulfatados de benzoxazoles sustituidos
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
BRPI0919816A2 (pt) * 2008-09-26 2019-09-24 Eisai R&D Man Co Ltd uso compostos benzoxazólicos no tratamento de malária
EP2350032B1 (en) * 2008-09-26 2016-05-25 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
CN107427517B (zh) * 2015-02-24 2021-11-16 国立大学法人鸟取大学 用于痴呆症的预防及/或治疗的医药
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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SU600138A1 (ru) * 1976-06-25 1978-03-30 Ленинградский Технологический Институт Имени Ленсовета Способ получени оксипроизводных 2-арилбензазолов
US4418068A (en) * 1981-04-03 1983-11-29 Eli Lilly And Company Antiestrogenic and antiandrugenic benzothiophenes
ATE227569T1 (de) * 1995-06-23 2002-11-15 Advanced Life Sciences Inc Robustaflavon und dessen derivate als antivirales mittel
US5998402A (en) * 1996-04-19 1999-12-07 American Home Products Corporation 2-phenyl-1-[4-(2-aminoethoxy)-benzyl]-indoles as estrogenic agents
US5948776A (en) * 1996-10-23 1999-09-07 Zymogenetic, Inc. Compositions and methods for treating bone deficit conditions
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CZ20013714A3 (cs) * 1999-04-16 2002-08-14 Astrazeneca Ab Léčivo pro léčení nemocí spojených s receptorem - beta estrogenu
WO2002046168A1 (en) * 2000-12-07 2002-06-13 Astrazeneca Ab Therapeutic benzimidazole compounds
JP2004524289A (ja) * 2000-12-22 2004-08-12 アストラゼネカ・アクチエボラーグ 治療化合物
WO2002056969A2 (en) * 2001-01-18 2002-07-25 Acumen Manufacturing Limited 10k step exercise method and apparatus
SG154323A1 (en) * 2001-03-16 2009-08-28 Wyeth Corp 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
CA2576353A1 (en) 2006-03-09
US20060046968A1 (en) 2006-03-02
EP1781628A2 (en) 2007-05-09
SV2006002205A (es) 2006-09-14
AU2005280178A1 (en) 2006-03-09
CN101044126A (zh) 2007-09-26
JP2008510827A (ja) 2008-04-10
GT200500228A (es) 2006-06-22
WO2006026316A3 (en) 2006-05-26
US20080255057A1 (en) 2008-10-16
RU2007105232A (ru) 2008-10-20
CR8931A (es) 2007-08-28
PE20060503A1 (es) 2006-07-20
CL2008000506A1 (es) 2008-06-13
BRPI0514628A (pt) 2008-06-17
NI200700055A (es) 2008-02-27
NO20071159L (no) 2007-03-26
KR20070046148A (ko) 2007-05-02
ECSP077279A (es) 2007-03-29
MX2007002251A (es) 2007-04-20
TW200612925A (en) 2006-05-01
IL181236A0 (en) 2007-07-04
WO2006026316A2 (en) 2006-03-09

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