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AR085666A1 - Derivados de c4-monometil triterpenoides y una composicion farmaceutica - Google Patents

Derivados de c4-monometil triterpenoides y una composicion farmaceutica

Info

Publication number
AR085666A1
AR085666A1 ARP120100803A ARP120100803A AR085666A1 AR 085666 A1 AR085666 A1 AR 085666A1 AR P120100803 A ARP120100803 A AR P120100803A AR P120100803 A ARP120100803 A AR P120100803A AR 085666 A1 AR085666 A1 AR 085666A1
Authority
AR
Argentina
Prior art keywords
alkyl
hydrogen
alkylamino
alkoxy
groups
Prior art date
Application number
ARP120100803A
Other languages
English (en)
Inventor
Christopher F Bender
Melean Visnick
Keith W Woods
Xian Jiang
Julie Miyashiro
Eric Anderson
Original Assignee
Reata Pharmaceuticals Inc
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 Reata Pharmaceuticals Inc filed Critical Reata Pharmaceuticals Inc
Publication of AR085666A1 publication Critical patent/AR085666A1/es

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07JSTEROIDS
    • C07J63/00Steroids in which the cyclopenta(a)hydrophenanthrene skeleton has been modified by expansion of only one ring by one or two atoms
    • C07J63/008Expansion of ring D by one atom, e.g. D homo steroids
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07JSTEROIDS
    • C07J63/00Steroids in which the cyclopenta(a)hydrophenanthrene skeleton has been modified by expansion of only one ring by one or two atoms
    • 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
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/18Drugs for disorders of the alimentary tract or the digestive system for pancreatic disorders, e.g. pancreatic enzymes
    • 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
    • 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
    • A61P17/00Drugs for dermatological disorders
    • A61P17/06Antipsoriatics
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    • A61P21/00Drugs for disorders of the muscular or neuromuscular system
    • A61P21/02Muscle relaxants, e.g. for tetanus or cramps
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    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P21/00Drugs for disorders of the muscular or neuromuscular system
    • A61P21/04Drugs for disorders of the muscular or neuromuscular system for myasthenia gravis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • AHUMAN NECESSITIES
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    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/08Antiepileptics; Anticonvulsants
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    • A61P25/00Drugs for disorders of the nervous system
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    • AHUMAN NECESSITIES
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    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/14Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • A61P25/16Anti-Parkinson drugs
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/18Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/24Antidepressants
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • 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
    • A61P27/00Drugs for disorders of the senses
    • A61P27/02Ophthalmic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00Drugs for disorders of the senses
    • A61P27/02Ophthalmic agents
    • A61P27/06Antiglaucoma agents or miotics
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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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    • 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
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    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P37/00Drugs for immunological or allergic disorders
    • 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
    • A61P37/06Immunosuppressants, e.g. drugs for graft rejection
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    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/08Antiallergic agents
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    • 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
    • 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07JSTEROIDS
    • C07J71/00Steroids in which the cyclopenta(a)hydrophenanthrene skeleton is condensed with a heterocyclic ring
    • C07J71/0005Oxygen-containing hetero ring

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

Abstract

Los compuestos de la presente son útiles en el tratamiento y prevención de enfermedades inflamatorias y proliferativas.Reivindicación 1: Un compuesto caracterizado porque es de la fórmula (1) donde: X1 y X2 son en forma independiente hidrógeno, halo, hidroxi, amino o oxo, con la condición de que X1 no es oxo cuando los átomos de carbono 12 y 13 están conectados entre sí con una unión doble, además con la condición de que X2 no es oxo cuando los átomos de carbono 9 y 11 están conectados entre sí con una unión doble; R1 es -H, -CN, halo, -CF3, o -C(O)Ra, donde Ra es -OH, alcoxi C1-4, -NH2, alquilamino C1-4, o -NH-S(O)2-alquilo C1-4; R2 es hidrógeno o R2 se encuentra ausente cuando el átomo al cual está unido forma parte de una unión doble; R2’ es hidrógeno, =CH2, alquilo C£8, o alquilo C£8 sustituido; R3 y R4 son en forma independiente entre sí hidrógeno, hidroxi, metilo o como se define más adelante cuando cualquiera de estos grupos se toma junto con el grupo Rc; e Y es: -H, -OH, -SH, -CN, -F, -CF3, -NH2 o -NCO; alquilo C£8, alquenilo C£8, alquinilo C£8, arilo C£12, aralquilo C£12, heteroarilo C£8, heterocicloalquilo C£12, alcoxi C£8, ariloxi C£12, aciloxi C£8, alquilamino C£8, dialquilamino C£8, alquenilamino C£8, arilamino C£8, aralquilamino C£8, alquiltio C£8, aciltio C£8, alquilsulfonilamino C£8, o versiones sustituidas de cualquiera de estos grupos; -alcanodiil C£8-Rb, -alquenodiil C£8-Rb, o una versión sustituida de cualquiera de estos grupos, donde Rb es: hidrógeno, hidroxi, halo, amino o tio; o heteroarilo C£8, alcoxi C£8, alqueniloxi C£8, ariloxi C£8, aralcoxi C£8, heteroariloxi C£8, aciloxi C£8, alquilamino C£8, dialquilamino C£8,alquenilamino C£8, arilamino C£8, aralquilamino C£8, heteroarilamino C£8, alquilsulfonilamino C£8, amido C£8, -OC(O)NH-alquilo C£8,-OC(O)CH2NHC(O)O-t-butilo, -OCH2-alquiltio C£8, o una versión sustituida de cualquiera de estos grupos; -(CH2)mC(O)Rc, donde m es 0 - 6 y Rc es: hidrógeno, hidroxi, halo, amino, -NHOH, un resto de fórmula (2) o tio; o alquilo C£8, alquenilo C£8, alquinilo C£8, arilo C£8, aralquilo C£8, heteroarilo C£8, heterocicloalquilo C£8, alcoxi C£8, alqueniloxi C£8, ariloxi C£8, aralcoxi C£8, heteroariloxi C£8, aciloxi C£8, alquilamino C£8, dialquilamino C£8, arilamino C£8, alquilsulfonilamino C£8, amido C£8, -NH-alcoxi C£8, -NH-heterocicloalquilo C£8, -NHC(NOH)-alquilo C£8, -NH-amido C£8, o una versión sustituida de cualquiera de estos grupos; Rc y R3, tomados juntos, son -O- o -NRd-, donde Rd es hidrógeno o alquilo C£4; o Rc y R4, tomados juntos, son -O- o -NRd-, donde Rd es hidrógeno o alquilo C£4; o -NHC(O)Re, donde Re es: hidrógeno, hidroxi, amino; o alquilo C£8, alquenilo C£8, alquinilo C£8, arilo C£8, aralquilo C£8, heteroarilo C£8,heterocicloalquilo C£8, alcoxi C£8, ariloxi C£8, aralcoxi C£8, heteroariloxi C£8, aciloxi C£8, alquilamino C£8, dialquilamino C£8, arilamino C£8, o una versión sustituida de cualquiera de estos grupos; o una sal farmacéuticamente aceptable o tautómero del mismo.
ARP120100803A 2011-03-11 2012-03-12 Derivados de c4-monometil triterpenoides y una composicion farmaceutica AR085666A1 (es)

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US201161452017P 2011-03-11 2011-03-11

Publications (1)

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AR085666A1 true AR085666A1 (es) 2013-10-16

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Country Link
US (1) US9290536B2 (es)
EP (1) EP2683731B1 (es)
JP (1) JP6129084B2 (es)
KR (1) KR101956399B1 (es)
CN (1) CN103619866B (es)
AR (1) AR085666A1 (es)
AU (1) AU2012229244B2 (es)
BR (1) BR112013023174B1 (es)
CA (1) CA2829618C (es)
CL (1) CL2013002612A1 (es)
CO (1) CO6801741A2 (es)
CY (1) CY1121744T1 (es)
DK (1) DK2683731T3 (es)
EA (1) EA026847B1 (es)
ES (1) ES2729405T3 (es)
HR (1) HRP20191164T1 (es)
HU (1) HUE044081T2 (es)
IL (1) IL228297B (es)
LT (1) LT2683731T (es)
ME (1) ME03469B (es)
MX (1) MX348862B (es)
PL (1) PL2683731T3 (es)
PT (1) PT2683731T (es)
RS (1) RS59200B1 (es)
SG (1) SG193404A1 (es)
SI (1) SI2683731T1 (es)
SM (1) SMT201900433T1 (es)
TR (1) TR201909788T4 (es)
TW (1) TWI535731B (es)
UY (1) UY33946A (es)
WO (1) WO2012125488A1 (es)

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