AR044649A1 - COMPUESTOS UTILES EN LA TERAPIA DE ENFERMEDADES QUE REQUIEREN LA INHIBICION DE UNA 17a - HIDROXIESTEROIDE - DEHIDROGENASA (17a- HSD) - Google Patents

COMPUESTOS UTILES EN LA TERAPIA DE ENFERMEDADES QUE REQUIEREN LA INHIBICION DE UNA 17a - HIDROXIESTEROIDE - DEHIDROGENASA (17a- HSD)

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Publication number
AR044649A1
AR044649A1 ARP040101982A ARP040101982A AR044649A1 AR 044649 A1 AR044649 A1 AR 044649A1 AR P040101982 A ARP040101982 A AR P040101982A AR P040101982 A ARP040101982 A AR P040101982A AR 044649 A1 AR044649 A1 AR 044649A1
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Argentina
Prior art keywords
alkyl
group
optionally substituted
cycle
alkylene group
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ARP040101982A
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English (en)
Inventor
Kristina Wahala
Annamaria Lilienkampf
Sari Alho
Kaisa Huhtinen
Nina Johansson
Pasi Koskimies
Kimmo Vihko
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Solvay Pharm Bv
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Publication of AR044649A1 publication Critical patent/AR044649A1/es

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    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D495/00Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
    • C07D495/02Heterocyclic 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
    • C07D495/04Ortho-condensed systems
    • 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
    • A61K31/495Heterocyclic 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
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • 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
    • A61K31/55Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00Drugs for disorders of the urinary system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00Drugs for disorders of the urinary system
    • A61P13/02Drugs for disorders of the urinary system of urine or of the urinary tract, e.g. urine acidifiers
    • 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
    • A61P13/12Drugs for disorders of the urinary system of the kidneys
    • 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
    • A61P15/10Drugs for genital or sexual disorders; Contraceptives for impotence
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • AHUMAN NECESSITIES
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    • A61P17/00Drugs for dermatological disorders
    • A61P17/02Drugs for dermatological disorders for treating wounds, ulcers, burns, scars, keloids, or the like
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    • A61P17/10Anti-acne agents
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    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • A61P17/14Drugs for dermatological disorders for baldness or alopecia
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    • 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
    • A61P19/00Drugs for skeletal disorders
    • A61P19/08Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • A61P19/10Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease for osteoporosis
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    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • 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
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    • A61P25/30Drugs for disorders of the nervous system for treating abuse or dependence
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    • A61P27/00Drugs for disorders of the senses
    • A61P27/02Ophthalmic agents
    • A61P27/12Ophthalmic agents for cataracts
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    • 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]
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    • A61P35/00Antineoplastic agents
    • A61P35/04Antineoplastic agents specific for metastasis
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    • A61P39/00General protective or antinoxious agents
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    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • A61P5/24Drugs for disorders of the endocrine system of the sex hormones
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    • A61P7/04Antihaemorrhagics; Procoagulants; Haemostatic agents; Antifibrinolytic agents
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D495/00Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
    • C07D495/12Heterocyclic 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 three hetero rings
    • C07D495/14Ortho-condensed systems

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Dermatology (AREA)
  • Urology & Nephrology (AREA)
  • Epidemiology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Rheumatology (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Endocrinology (AREA)
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  • Psychiatry (AREA)
  • Ophthalmology & Optometry (AREA)
  • Diabetes (AREA)
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  • Hematology (AREA)
  • Oncology (AREA)
  • Gynecology & Obstetrics (AREA)
  • Hospice & Palliative Care (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
  • Steroid Compounds (AREA)

Abstract

Compuestos útiles en la terapia, especialmente para el tratamiento y/o prevención de una afección dependiente de una hormona esteroide, preferiblemente una enfermedad o afección dependiente de una hormona esteroide que requiere la inhibición de una 17b-hidroxiesteroide-dehidrogenasa (17b-HSD) tal como enzima 17b-HSD tipo 1, tipo 2 o tipo 3. Reivindicación 3: Compuestos de la fórmula (1), en la cual: R1 y R2 representan radicales C1-8-alquilo, iguales o distintos entre sí o uno de ellos es C1- 8-alquilo y el otro es H; o R1 y R2 forman conjuntamente con los átomos de carbonos a los cuales están ligados un sistema cíclico de 5-, 6-, 7- u 8 miembros, saturado o que contiene uno o más dobles ligaduras entre los átomos del cíclico, conteniendo dicho ciclo opcionalmente hasta dos átomos de nitrógeno en adición al átomo de nitrógeno al que está fijado R1, estando dicho ciclo opcionalmente sustituido con hasta dos sustituyentes independientemente elegidos del grupo que comprende alquilo, alquilo sustituido, arilo, o arilalquilo, cuyo radical arilo está opcionalmente sustituido, alcoxi, ariloxi, aciloxi, ariltio, alquiltio, arilsulfonilo, alquilsulfonilo, hidroxilo, oxo, halógeno, amino, oxima, acilo, tiocarboxilo y amido; la cadena de hidrocarburo -C(R5)-C(R6)C(CH)n- del sistema cíclico adyacente al ciclo tiofeno es saturada o contiene una o más dobles ligaduras entre los átomos de carbono; n es un número de 1 a 4; y R5 y R6 están individualmente elegidos del grupo que comprende hidrógeno, alquilo, alquilo sustituido, arilo o arilquilo, cuyo radical arilo está opcionalmente sustituido, alcoxi, ariloxi, aciloxi, ariltio, alquiltio, arilsulfonilo, alquilsulfonilo, hidroxilo, oxo, halógeno, amino, oxima, acilo, carboxilo, tiocarboxilo, y amido; con la condición que en el caso en que n representa los números 1, 2 ó 3, y R1 y R2 están independientemente seleccionados del grupo que comprende hidrógeno, o C1-4-alquilo o que en conjunto forman un grupo alquileno no sustituido de tres a cinco grupos metileno o un grupo imino-alquileno de dos a cuatro grupos metileno en el grupo alquileno, opcionalmente sustituido en el átomo de N, entonces al menos R5 o R6 debe ser distinto de hidrógeno, C1-4- alquilo o alquilcarboxilo, o la cadena de hidrocarburo C(R5)C(R6)-(CH)n del sistema cíclico adyacente al ciclo tiofeno debe ser insaturado o aromática; en el caso en que n representa 2 y R1-R2 forman un grupo alquileno no sustituido de 3 a 5 grupos metileno, entonces R6 debe ser distinto de bromo, dibromo o feniltio, si R5 representa un grupo hidroxilo u oxo; o en el caso en que n representa 2 y R1-R2 forman un grupo pentametileno no sustituido, R5 deber ser distinto de feniltio si R6 representa carbonilo, para uso en terapia.
ARP040101982A 2003-06-10 2004-06-08 COMPUESTOS UTILES EN LA TERAPIA DE ENFERMEDADES QUE REQUIEREN LA INHIBICION DE UNA 17a - HIDROXIESTEROIDE - DEHIDROGENASA (17a- HSD) AR044649A1 (es)

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US47701703P 2003-06-10 2003-06-10

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AR044649A1 true AR044649A1 (es) 2005-09-21

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US (3) US7754709B2 (es)
EP (1) EP1635840B1 (es)
JP (1) JP4612628B2 (es)
CN (1) CN100502876C (es)
AR (1) AR044649A1 (es)
AT (1) ATE401893T1 (es)
AU (1) AU2004246791B2 (es)
BR (1) BRPI0411319A (es)
CA (1) CA2527591A1 (es)
DE (1) DE602004015287D1 (es)
DK (1) DK1635840T3 (es)
ES (1) ES2311156T3 (es)
PL (1) PL1635840T3 (es)
PT (1) PT1635840E (es)
SA (1) SA04250158B1 (es)
TW (1) TW200504078A (es)
WO (1) WO2004110459A1 (es)

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AU2004246791A1 (en) 2004-12-23
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ATE401893T1 (de) 2008-08-15
US20050032778A1 (en) 2005-02-10
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EP1635840B1 (en) 2008-07-23
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