AR096728A1 - Derivados de estratrieno-tiazol terapéuticamente activos - Google Patents

Derivados de estratrieno-tiazol terapéuticamente activos

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Publication number
AR096728A1
AR096728A1 ARP140102398A ARP140102398A AR096728A1 AR 096728 A1 AR096728 A1 AR 096728A1 AR P140102398 A ARP140102398 A AR P140102398A AR P140102398 A ARP140102398 A AR P140102398A AR 096728 A1 AR096728 A1 AR 096728A1
Authority
AR
Argentina
Prior art keywords
alkyl
group
perhaloalkyl
independently selected
halogen
Prior art date
Application number
ARP140102398A
Other languages
English (en)
Original Assignee
Forendo Pharma Ltd
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 Forendo Pharma Ltd filed Critical Forendo Pharma Ltd
Publication of AR096728A1 publication Critical patent/AR096728A1/es

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Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J71/00—Steroids in which the cyclopenta(a)hydrophenanthrene skeleton is condensed with a heterocyclic ring
    • C07J71/0036—Nitrogen-containing hetero ring
    • C07J71/0057—Nitrogen and oxygen
    • C07J71/0063—Nitrogen and oxygen at position 2(3)
    • 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
    • A61K31/56—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
    • A61K31/58—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids containing heterocyclic rings, e.g. danazol, stanozolol, pancuronium or digitogenin
    • 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
    • A61K31/70—Carbohydrates; Sugars; Derivatives thereof
    • A61K31/7028—Compounds having saccharide radicals attached to non-saccharide compounds by glycosidic linkages
    • A61K31/7034—Compounds having saccharide radicals attached to non-saccharide compounds by glycosidic linkages attached to a carbocyclic compound, e.g. phloridzin
    • A61K31/704—Compounds having saccharide radicals attached to non-saccharide compounds by glycosidic linkages attached to a carbocyclic compound, e.g. phloridzin attached to a condensed carbocyclic ring system, e.g. sennosides, thiocolchicosides, escin, daunorubicin
    • 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
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • A61P15/08—Drugs for genital or sexual disorders; Contraceptives for gonadal disorders or for enhancing fertility, e.g. inducers of ovulation or of spermatogenesis
    • 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
    • A61P19/00—Drugs for skeletal disorders
    • 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
    • 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
    • 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
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/04—Anorexiants; Antiobesity agents
    • 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
    • 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
    • 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
    • A61P5/28—Antiandrogens
    • 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
    • A61P5/32—Antioestrogens
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J43/00—Normal steroids having a nitrogen-containing hetero ring spiro-condensed or not condensed with the cyclopenta(a)hydrophenanthrene skeleton
    • C07J43/003—Normal steroids having a nitrogen-containing hetero ring spiro-condensed or not condensed with the cyclopenta(a)hydrophenanthrene skeleton not condensed
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J51/00—Normal steroids with unmodified cyclopenta(a)hydrophenanthrene skeleton not provided for in groups C07J1/00 - C07J43/00
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J71/00—Steroids in which the cyclopenta(a)hydrophenanthrene skeleton is condensed with a heterocyclic ring
    • C07J71/0036—Nitrogen-containing hetero ring
    • C07J71/0057—Nitrogen and oxygen

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Public Health (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Epidemiology (AREA)
  • Endocrinology (AREA)
  • Diabetes (AREA)
  • Urology & Nephrology (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Neurosurgery (AREA)
  • Molecular Biology (AREA)
  • Ophthalmology & Optometry (AREA)
  • Rheumatology (AREA)
  • Reproductive Health (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Gynecology & Obstetrics (AREA)
  • Psychiatry (AREA)
  • Immunology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Pain & Pain Management (AREA)
  • Hospice & Palliative Care (AREA)
  • Pregnancy & Childbirth (AREA)
  • Obesity (AREA)
  • Dermatology (AREA)
  • Hematology (AREA)
  • Child & Adolescent Psychology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Steroid Compounds (AREA)

Abstract

La presente se refiere a los compuestos de la fórmula (1) y sus sales farmacéuticamente aceptables. La presente se refiere asimismo a su utilización como inhibidores de 17b-HSD1 y en el tratamiento o la prevención de enfermedades o trastornos dependientes de las hormonas esteroides, tales como enfermedades o trastornos dependientes de las hormonas esteroides que requieren la inhibición de la enzima 17b-HSD1 y/o que requieren la disminución de la concentración de estradiol endógeno. La presente también se refiere a la preparación de los compuestos antes mencionados y a composiciones farmacéuticas que comprenden como ingrediente(s) activo(s) uno o más de los compuestos antes mencionados o sales farmacéuticamente aceptables de los mismos. Reivindicación 1: Un compuesto de fórmula (1) en donde (i) R¹ se selecciona del grupo integrado por H, NO₂, OH y N(R)₂; (ii-a) R² y R⁴ se seleccionan cada uno independientemente del grupo integrado por H, halógeno, alquilo-C₁₋₆, haloalquilo-C₁₋₃, perhaloalquilo-C₁₋₃, CN, NO₂, N₃, N(R)₂, (-CH₂)ₙN(R)₂, OR, (CH₂)ₙOR, CO₂R, CONHR, NHCOR, C(=NH)R, C(=N-OH)R y COR; y R³ se selecciona del grupo integrado por H, alquilo-C₁₋₆, haloalquilo-C₁₋₃, perhaloalquilo-C₁₋₆, N(R)₂, N₃ y OR³, en donde R³ se selecciona del grupo integrado por R, bencilo, succinilo, glucuronilo opcionalmente acilado, (CH₂)ₙOH, SO₂OH, SO₂R, tosilo, SO₂N(R)₂, PO(OR)₂, COOR, C(O)N(R)₂, C(O)(CH₂)ₙN(R)₂, C(O)CH₂NHC(O)R, C(O)CH₂NHC(O)OR y C(O)R; o (ii-b) R² y R³ o R³ y R⁴, junto con los átomos de carbono del anillo a los cuales están unidos, forman un anillo heterocíclico insaturado o aromático de 5 miembros que comprende 1 ó 2 heteroátomos, cada uno seleccionado independientemente de N y O, opcionalmente sustituido con metilo u oxo; y R⁴ o R², respectivamente, es H y halógeno; (iii) R⁵ y R⁶ se seleccionan cada uno independientemente del grupo integrado por H, halógeno,-OH, alcoxi-C₁₋₃ y CHO, o R⁵ y R⁶ forman juntos =CH-OH; R es H o alquilo-C₁₋₆, haloalquilo-C₁₋₃, o perhaloalquilo-C₁₋₃, o cuando es parte de algún N(R)₂, ambos R junto con el nitrógeno al cual están unidos pueden formar un anillo heterocíclico alifático o aromático de 5 a 6 miembros que comprende 1 ó 2 heteroátomos, cada uno seleccionado independientemente de N y O; R es alquilo-C₁₋₆, haloalquilo-C₁₋₃ o perhaloalquilo-C₁₋₃; R es alquilo-C₁₋₁₈, alquenilo-C₂₋₁₈, -(CH₂)ₙ-cicloalquilo-C₃₋₆, o fenilo opcionalmente sustituido; y n es 1 ó 2; o con la condición deque cuando R¹, R², R⁴, R⁵ y R⁶ son cada uno H, R³ no es OH o metoxi; o una sal farmacéuticamente aceptable del mismo.
ARP140102398A 2013-06-25 2014-06-25 Derivados de estratrieno-tiazol terapéuticamente activos AR096728A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
FI20135693 2013-06-25

Publications (1)

Publication Number Publication Date
AR096728A1 true AR096728A1 (es) 2016-01-27

Family

ID=51220583

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP140102398A AR096728A1 (es) 2013-06-25 2014-06-25 Derivados de estratrieno-tiazol terapéuticamente activos

Country Status (7)

Country Link
US (1) US10377791B2 (es)
EP (1) EP3013845B1 (es)
JP (1) JP6461127B2 (es)
CN (1) CN105518016B (es)
AR (1) AR096728A1 (es)
TW (1) TW201512215A (es)
WO (1) WO2014207309A1 (es)

Families Citing this family (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US9320528B2 (en) * 2013-06-26 2016-04-26 Misonix, Incorporated Ultrasonic cutting blade with cooling liquid conduction
EP3237431B1 (en) 2014-12-23 2019-03-20 Forendo Pharma Ltd Prodrugs of 17.beta.-hsd1 -inhibitors
CZ307437B6 (cs) 2016-06-07 2018-08-22 Ăšstav organickĂ© chemie a biochemie AV ÄŚR, v.v.i. 15β-substituované deriváty estronu jako selektivní inhibitory 17β-hydroxysteoiddehydrogenáz
NZ760155A (en) * 2017-06-08 2022-09-30 Forendo Pharma Ltd 15.beta.-[3-propanamido]-substituted estra-1,3,5
EP3891167A1 (en) 2018-12-05 2021-10-13 Forendo Pharma Ltd Estra-1,3,5(10)-triene compounds condensed in position 16(17) with a pyrazole ring as inhibitors of 17-hsd1

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AU2707999A (en) 1998-03-11 1999-09-27 Endorecherche Inc. Inhibitors of type 5 and type 3 17beta-hydroxysteroid dehydrogenase and methods for their use
WO2000007996A2 (en) 1998-08-07 2000-02-17 Chiron Corporation Pyrazoles as estrogen receptor modulators
GB9929302D0 (en) 1999-12-11 2000-02-02 Univ Cardiff Benzyl tetralins compositions and uses thereof
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Also Published As

Publication number Publication date
CN105518016A (zh) 2016-04-20
JP6461127B2 (ja) 2019-01-30
WO2014207309A1 (en) 2014-12-31
TW201512215A (zh) 2015-04-01
EP3013845A1 (en) 2016-05-04
CN105518016B (zh) 2020-10-23
US20170114090A1 (en) 2017-04-27
US10377791B2 (en) 2019-08-13
JP2016523885A (ja) 2016-08-12
EP3013845B1 (en) 2020-03-18

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