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AR047144A1 - Derivados de 1-n-fenilamino-1h-imidazol y composiciones farmaceuticas que los contienen - Google Patents

Derivados de 1-n-fenilamino-1h-imidazol y composiciones farmaceuticas que los contienen

Info

Publication number
AR047144A1
AR047144A1 ARP040104657A ARP040104657A AR047144A1 AR 047144 A1 AR047144 A1 AR 047144A1 AR P040104657 A ARP040104657 A AR P040104657A AR P040104657 A ARP040104657 A AR P040104657A AR 047144 A1 AR047144 A1 AR 047144A1
Authority
AR
Argentina
Prior art keywords
scsnr10
tetrazolyl
scsnr10r11
sconr10r11
oso2or10
Prior art date
Application number
ARP040104657A
Other languages
English (en)
Original Assignee
Theramex
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
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=34702365&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=AR047144(A1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Priority claimed from EP03293152A external-priority patent/EP1544195A1/en
Application filed by Theramex filed Critical Theramex
Publication of AR047144A1 publication Critical patent/AR047144A1/es

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D233/00Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
    • C07D233/54Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members
    • 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
    • A61K31/41641,3-Diazoles
    • 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
    • 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
    • A61P15/08Drugs for genital or sexual disorders; Contraceptives for gonadal disorders or for enhancing fertility, e.g. inducers of ovulation or of spermatogenesis
    • 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
    • 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
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/02Immunomodulators
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00Drugs for disorders of the endocrine system
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D409/00Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/02Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
    • C07D409/12Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D419/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen, oxygen, and sulfur atoms as the only ring hetero atoms
    • C07D419/02Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen, oxygen, and sulfur atoms as the only ring hetero atoms containing two hetero rings
    • C07D419/12Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen, oxygen, and sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Reproductive Health (AREA)
  • Endocrinology (AREA)
  • Neurosurgery (AREA)
  • Gynecology & Obstetrics (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Immunology (AREA)
  • Pregnancy & Childbirth (AREA)
  • Psychiatry (AREA)
  • Hospice & Palliative Care (AREA)
  • Diabetes (AREA)
  • Urology & Nephrology (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)

Abstract

Se refiere a compuestos y a las composiciones farmacéuticas que contienen a estos compuestos. utiles como inhibidores de la enzima aromatasa. Reivindicacion 1: Un derivado de imidazol de formula (1), y sales de adicion de ácidos y formas estereoisomeras del mismo, en donde: R1 y R2 son cada uno independientemente hidrogeno, un alquilo C1-6 o un cicloalquilo C3-8; o R1 y R2 juntos forman un anillo carbocíclico de 5, 6 o 7 miembros, saturado o insaturado; Q es (CH2)m-X-(CH2)n-A; A es un enlace directo, O, S, SO, SO2, NR5; X es un enlace directo, CF2, O, S, SO, SO2, C(O), NR5 o CR6R7; Z es un grupo seleccionado entre las formulas (2) a (8); m y n son cada uno independientemente 0, 1, 2, 3 o 4; p es 1, 2, 3 o 4; q es 0, 1 o 2; la línea de puntos significa que R8 y/o R9 pueden estar en cualquier posicion del anillo benzotiofeno; R3 y R8 son cada uno independientemente hidrogeno o un grupo hidroxi, ciano, halogeno, nitro, alquilo C1-6, alcoxi C1-6, trifluorometilo, alquiltio C1-6, alquilsulfonilo C1-6, acilo, alcoxicarbonilo C1-6, carboxamido, OPO(OR10)2, NR10R11, SO2NR10R11, OSO2NR10R11, OSO2OR10, SO2OR10, SSO2NR10R11, CF2SO2OR10, CF2SO2NR10R11, CF2-tetrazolilo o NR12SO2NR10R11, OSO2NR10SO2NR11R12, CO2R10, CONR10R11, OCHO, OCONR10R11, OCSNR10R11, SCONR10R11, SCSNR10R11, tetrazolilo, NR12CONR10R11, NR10-CHO; cuando Q-Z es un grupo de formula (9), n es 0, 1 o 2 y p es 1, uno de R3 y R8 es un grupo hidroxi, nitro, OPO(OR10)2, NR10R11, OSO2NR10R11, OSO2OR10, SO2OR10, SSO2NR10R11, CF2SO2OR10, CF2SO2NR10R11, CF2-tetrazolilo o NR12SO2NR10R11, OSO2NR10SO2NR11R12, CO2R10, CONR10R11, OCHO, OCONR10R11, OCSNR10R11, SCONR10R11, SCSNR10R11, tetrazolilo, NR12CONR10R11, NR10-CHO y el otro es hidrogeno o un grupo hidroxi, ciano, halogeno, nitro, alquilo C1-6, alcoxi C1-6, trifluorometilo, alquiltio C1-6, alquilsulfonilo C1-6, acilo, alcoxicarbonilo C1-6, carboxamido, NR10R11, SO2NR10R11, OSO2NR10R11, OSO2OR10, SO2OR10, SSO2NR10R11, CF2SO2OR10, CF2SO2NR10R11, CF2-tetrazolilo o NR12SO2NR10R11, OSO2NR12SO2NR10R11, CO2R10, CONR10R11, OCHO, OCONR10R11, OCSNR10R11, SCONR10R11, SCSNR10R11, tetrazolilo, NR12CONR10R11, NR10-CHO; R4 y R9 son cada uno independientemente hidrogeno o un grupo hidroxi, ciano, halogeno, nitro, OPO(OR10)2, alquilo C1-6, alcoxi C1-6, trifluorometilo, alquiltio C1-6, alquilsulfonilo C1-6, acilo, alcoxicarbonilo C1-6, carboxamido, NR10R11, SO2NR10R11, OSO2NR10R11, OSO2OR10, SO2OR10, SSO2NR10R11, CF2SO2OR10, CF2SO2NR10R11, CF2- tetrazolilo o NR12SO2NR10R11, OSO2NR12SO2NR10R11, CO2R10, CHO, CONR10R11, OCHO, OCONR10R11, OCSNR10R11, SCONR10R11, SCSNR10R11, tetrazolilo, NR12CONR10R11, NR10-CHO; cuando p es 2, 3 o 4, los R9 pueden ser iguales o diferentes; R6 y R7 son independientemente hidrogeno, halogeno, un alquilo C1-6 o un cicloalquilo C3-8; R5, R10, R11 y R12 son cada uno independientemente hidrogeno, hidroxi, un alquilo C1-6 o un cicloalquilo C3-8; R10 puede ser también una sal; R10 y R11 pueden formar también, junto con el átomo de nitrogeno al cual están unidos, un heterociclo de 5 a 7 miembros que contiene uno o dos heteroátomos seleccionados entre O, S y N; cuando Z es una formula (10), y p es 1: a) R8 y R9 pueden formar también junto con el anillo fenilo un dioxido de benzoxatiazina, un dioxido de dihidrobenzoxatiazina, un dioxido de benzoxatiazinona, un dioxido de benzoxatiazol, un tetraoxido de benzoxaditiadiazina, un tetraoxido de benzoditiazina o un tetraoxido de benzodioxaditina; b) R3 y R4 junto con el anillo fenilo que los lleva también puede formar un benzofurano o un N-metilbenzotriazol y luego R8 y R9 son independientemente un grupo hidroxi, nitro, OPO(OR10)2, NR10R11, OSO2NR10R11, OSO2OR10, SO2OR10, SSO2NR10R11, CF2SO2OR10, CF2SO2NR10R11, CF2-tetrazolilo o NR12SO2NR10R11, OSO2NR12SO2NR10R11, CO2R10, CONR10R11, OCHO, OCONR10R11, OCSNR10R11, SCONR10R11, SCSNR10R11, tetrazolilo, NR12CONR10R11, NR10-CHO.
ARP040104657A 2003-12-15 2004-12-15 Derivados de 1-n-fenilamino-1h-imidazol y composiciones farmaceuticas que los contienen AR047144A1 (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
EP03293152A EP1544195A1 (en) 2003-12-15 2003-12-15 1-N-phenyl-amino- 1H-imidazole derivatives and pharmaceutical compositions containing them
EP04292681 2004-11-12

Publications (1)

Publication Number Publication Date
AR047144A1 true AR047144A1 (es) 2006-01-11

Family

ID=34702365

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP040104657A AR047144A1 (es) 2003-12-15 2004-12-15 Derivados de 1-n-fenilamino-1h-imidazol y composiciones farmaceuticas que los contienen

Country Status (18)

Country Link
US (1) US8476455B2 (es)
EP (1) EP1694650A1 (es)
JP (2) JP4834557B2 (es)
KR (1) KR20060123186A (es)
CN (1) CN1890221B (es)
AR (1) AR047144A1 (es)
AU (1) AU2004299286B2 (es)
BR (1) BRPI0417407A (es)
CA (1) CA2549603A1 (es)
IL (1) IL176077A0 (es)
MA (1) MA28286A1 (es)
MX (1) MXPA06006837A (es)
NO (1) NO20062710L (es)
NZ (1) NZ548399A (es)
OA (1) OA13336A (es)
RU (1) RU2365586C2 (es)
TW (1) TW200533668A (es)
WO (1) WO2005058842A1 (es)

Families Citing this family (9)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB0127923D0 (en) 2001-11-21 2002-01-16 Sterix Ltd Compound
AU2007271486A1 (en) * 2006-07-05 2008-01-10 Merck Patent Gmbh Sulfamate benzothiophene derivatives
WO2008067892A1 (de) * 2006-12-04 2008-06-12 Merck Patent Gmbh Sulfamat-benzothiophen-derivate
BRPI0817045A2 (pt) 2007-09-17 2015-03-24 Preglem Sa Tratamento de condições estrogênio-dependentes em mulheres pré-menopáusicas
GB0914767D0 (en) 2009-08-24 2009-09-30 Sterix Ltd Compound
CA3008020C (en) 2015-12-09 2024-02-20 The Board Of Trustees Of The University Of Illinois Benzothiophene-based selective estrogen receptor downregulators
IL267795B2 (en) 2017-01-06 2023-02-01 G1 Therapeutics Inc Combination therapy for the treatment of cancer
WO2018187414A1 (en) * 2017-04-05 2018-10-11 The Regents Of The University Of California Inhibitors of mtor-rictor interactions
EP3801221A4 (en) * 2018-06-11 2022-03-30 Loma Linda University Methods of delaying and reversing alzheimer's disease progression

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Also Published As

Publication number Publication date
US8476455B2 (en) 2013-07-02
MA28286A1 (fr) 2006-11-01
AU2004299286A1 (en) 2005-06-30
CN1890221B (zh) 2014-07-16
CA2549603A1 (en) 2005-06-30
NO20062710L (no) 2006-06-30
JP4834557B2 (ja) 2011-12-14
WO2005058842A1 (en) 2005-06-30
AU2004299286B2 (en) 2011-06-30
RU2006125417A (ru) 2008-01-27
BRPI0417407A (pt) 2007-04-03
TW200533668A (en) 2005-10-16
JP2011190277A (ja) 2011-09-29
JP2007515420A (ja) 2007-06-14
JP5209760B2 (ja) 2013-06-12
US20070112009A1 (en) 2007-05-17
NZ548399A (en) 2011-01-28
OA13336A (en) 2006-04-13
MXPA06006837A (es) 2006-09-04
IL176077A0 (en) 2006-10-05
KR20060123186A (ko) 2006-12-01
EP1694650A1 (en) 2006-08-30
RU2365586C2 (ru) 2009-08-27
CN1890221A (zh) 2007-01-03

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