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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    • 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
    • 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
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • 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
    • A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/02—Drugs for disorders of the urinary system of urine or of the urinary tract, e.g. urine acidifiers
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/08—Drugs for disorders of the urinary system of the prostate
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/12—Drugs for disorders of the urinary system of the kidneys
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • A61P15/10—Drugs for genital or sexual disorders; Contraceptives for impotence
    • 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
    • A61P17/02—Drugs for dermatological disorders for treating wounds, ulcers, burns, scars, keloids, or the like
    • 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
    • A61P17/08—Antiseborrheics
    • 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
    • A61P17/10—Anti-acne agents
    • 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
    • A61P17/14—Drugs for dermatological disorders for baldness or alopecia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • A61P19/10—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease for osteoporosis
    • 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
    • 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
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/30—Drugs for disorders of the nervous system for treating abuse or dependence
    • 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
    • A61P27/12—Ophthalmic agents for cataracts
    • 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
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A61P35/04—Antineoplastic agents specific for metastasis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P39/00—General protective or antinoxious agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • 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
    • A61P5/00—Drugs for disorders of the endocrine system
    • A61P5/24—Drugs for disorders of the endocrine system of the sex hormones
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A61P7/04—Antihaemorrhagics; Procoagulants; Haemostatic agents; Antifibrinolytic agents
    • 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
    • C07D495/12—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 three hetero rings
    • C07D495/14—Ortho-condensed systems

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Dermatology (AREA)
  • Rheumatology (AREA)
  • Urology & Nephrology (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Epidemiology (AREA)
  • Biomedical Technology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Endocrinology (AREA)
  • Psychiatry (AREA)
  • Ophthalmology & Optometry (AREA)
  • Diabetes (AREA)
  • Reproductive Health (AREA)
  • Hospice & Palliative Care (AREA)
  • Addiction (AREA)
  • Immunology (AREA)
  • Pain & Pain Management (AREA)
  • Oncology (AREA)
  • Toxicology (AREA)
  • Gynecology & Obstetrics (AREA)
  • Hematology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Steroid Compounds (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (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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ARP040101982A AR044649A1 (es) 2003-06-10 2004-06-08 COMPUESTOS UTILES EN LA TERAPIA DE ENFERMEDADES QUE REQUIEREN LA INHIBICION DE UNA 17a - HIDROXIESTEROIDE - DEHIDROGENASA (17a- HSD)

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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)
HK (1) HK1087331A1 (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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CN110945007B (zh) 2017-06-08 2022-11-18 佛恩多制药有限公司 用于抑制17β-羟基类固醇脱氢酶的15β-[3-丙酰氨基]-取代的雌-1,3,5(10)-三烯-17-酮化合物及其17-肟
KR20200062314A (ko) 2017-10-11 2020-06-03 리제너론 파마슈티칼스 인코포레이티드 Pnpla3 i148m 변이를 발현하는 환자의 간 질환의 치료에서의 hsd17b13의 저해
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US20100249106A1 (en) 2010-09-30
TW200504078A (en) 2005-02-01
JP4612628B2 (ja) 2011-01-12
US20080103131A1 (en) 2008-05-01
WO2004110459A1 (en) 2004-12-23
AU2004246791A1 (en) 2004-12-23
SA04250158B1 (ar) 2007-10-29
US7754709B2 (en) 2010-07-13
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EP1635840B1 (en) 2008-07-23
HK1087331A1 (en) 2006-10-13
AU2004246791B2 (en) 2010-02-18
PT1635840E (pt) 2008-09-17
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ES2311156T3 (es) 2009-02-01
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DE602004015287D1 (en) 2008-09-04
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CN100502876C (zh) 2009-06-24
US20050032778A1 (en) 2005-02-10

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