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AR059216A1 - 11b-hidroxiandrosta-4-eno-3-onas - Google Patents

11b-hidroxiandrosta-4-eno-3-onas

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Publication number
AR059216A1
AR059216A1 ARP070100355A ARP070100355A AR059216A1 AR 059216 A1 AR059216 A1 AR 059216A1 AR P070100355 A ARP070100355 A AR P070100355A AR P070100355 A ARP070100355 A AR P070100355A AR 059216 A1 AR059216 A1 AR 059216A1
Authority
AR
Argentina
Prior art keywords
alkyl
cycloalkyl
oco
halogen
aryl
Prior art date
Application number
ARP070100355A
Other languages
English (en)
Inventor
Jiten Ranchlodbhal Patel
Gopalkumar Chimanial Patel
Samir Rameshchandra Shah
Sanjay Nandial Manhane
Trinadha R Chitturi
Gaurav Sanjivkumar Sheth
Original Assignee
Sun Pharmaceutical Ind 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 Sun Pharmaceutical Ind Ltd filed Critical Sun Pharmaceutical Ind Ltd
Publication of AR059216A1 publication Critical patent/AR059216A1/es

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07JSTEROIDS
    • C07J31/00Normal steroids containing one or more sulfur atoms not belonging to a hetero ring
    • C07J31/006Normal steroids containing one or more sulfur atoms not belonging to a hetero ring not covered by C07J31/003
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07JSTEROIDS
    • C07J31/00Normal steroids containing one or more sulfur atoms not belonging to a hetero ring
    • 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
    • A61P11/00Drugs for disorders of the respiratory system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • A61P11/06Antiasthmatics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • A61P17/04Antipruritics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • A61P17/06Antipsoriatics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • 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
    • A61P27/16Otologicals
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • 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]
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/04Anorexiants; Antiobesity agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • 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
    • 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/08Antiallergic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00Drugs for disorders of the endocrine system
    • A61P5/24Drugs for disorders of the endocrine system of the sex hormones
    • A61P5/30Oestrogens
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07JSTEROIDS
    • C07J17/00Normal steroids containing carbon, hydrogen, halogen or oxygen, having an oxygen-containing hetero ring not condensed with the cyclopenta(a)hydrophenanthrene skeleton
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07JSTEROIDS
    • C07J3/00Normal steroids containing carbon, hydrogen, halogen or oxygen, substituted in position 17 beta by one carbon atom
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    • C07ORGANIC CHEMISTRY
    • C07JSTEROIDS
    • C07J3/00Normal steroids containing carbon, hydrogen, halogen or oxygen, substituted in position 17 beta by one carbon atom
    • C07J3/005Normal steroids containing carbon, hydrogen, halogen or oxygen, substituted in position 17 beta by one carbon atom the carbon atom being part of a carboxylic function
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07JSTEROIDS
    • C07J41/00Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring
    • C07J41/0033Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring not covered by C07J41/0005
    • C07J41/0038Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring not covered by C07J41/0005 with an androstane skeleton, including 18- or 19-substituted derivatives, 18-nor derivatives and also derivatives where position 17-beta is substituted by a carbon atom not directly bonded to a further carbon atom and not being part of an amide group
    • 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
    • C07J71/001Oxiranes
    • C07J71/0015Oxiranes at position 9(11)

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Animal Behavior & Ethology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
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  • Pharmacology & Pharmacy (AREA)
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  • Bioinformatics & Cheminformatics (AREA)
  • Immunology (AREA)
  • Diabetes (AREA)
  • Pulmonology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Dermatology (AREA)
  • Rheumatology (AREA)
  • Obesity (AREA)
  • Endocrinology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Hematology (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Pain & Pain Management (AREA)
  • Emergency Medicine (AREA)
  • Ophthalmology & Optometry (AREA)
  • Transplantation (AREA)
  • Child & Adolescent Psychology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Steroid Compounds (AREA)

Abstract

Los compuestos reivindicados son potentes glucocorticoides antiinflamatorios ya que poseen una union selectiva hacia el receptor glucocorticoide. Reivindicacion 1: 11beta-hidroxiandrosta-4-eno-3-ona, compuesto de la formula (1), y la sal fisiologicamente aceptable del mismo: ------ representa una union simple o doble y representa la configuracion alfa o beta. En donde: Z representa O o S; R1 representa hidrogeno o metilo que puede estar ya sea en la configuracion alfa o beta, o metileno; R2 y R3 son lo mismo, o difieren y cada uno independientemente representa hidrogeno, halogeno o un grupo metilo; R5 representa un grupo seleccionado de alquilo C1-10, cicloalquilo C3-13, -O-alquilo C1-10, arilo o anillo heterocíclico en donde el anillo o sistema de anillo se encuentra sustituido o no sustituido por uno o más de entre halogeno, -OH, alquilo C1-3, -O-alquilo C1-3, cicloalquilo C3-13; en donde los grupos alquilo o cicloalquilo pueden contener opcionalmente una o más no saturaciones y/o puede tener uno o más heteroátomos incorporados en el mismo y opcionalmente en cada caso tener uno o más átomos de hidrogeno reemplazados por halogeno, -OH, alquilo C1-3, -O-alquilo C1-3, cicloalquilo C3-13; y R4 representa porcion seleccionada de un grupo que consiste de A, B y C, con la salvedad de que cuando R4 representa la porcion (C), Z es S, en donde m1 es 1, 2 o 3; m2 es 0 o 1; m3 es 0 o1; n1 es 0, 1 o2; R6 representa un grupo seleccionado de alquilo C1-8, cicloalquilo C3-13, arilo y un radical heterocíclico, donde el anillo o sistema de anillo se encuentra no sustituido o sustituido por uno o más sustituyentes seleccionados de alquilo C1-8, cicloalquilo C3-13, halogeno, O-alquilo C1-8, O-cicloalquilo C3-13, OCO-alquilo C1-3, S(O)0-2)-alquilo C1-8, COO-alquilo C1-8, -OCO-O-alquilo C1-3, -OCO-CO-O-alquilo C1-3, CONH2, CONH-alquilo C1-8, CON-[(alquilo C1-8]2, -NHCO-alquilo C1-8, N-alquilo C1-8-CO-alquilo C1-8, -NHCO-O-alquilo C1-8, -N-alquilo C1-8- CO-O-alquilo C1-8, -NHCONH-alquilo C1-8, -N-alquilo C1-8-CONH-alquilo C1-8, -NHCONH-SO2-alquilo C1-8, -N-alquilo C1-8-CONH-SO2-alquilo C1-8, -NO2, -CN; en donde los grupos alquilo o cicloalquilo pueden contener opcionalmente una o más no saturaciones y/o pueden tener uno o más heteroátomos incorporados en el mismo y opcionalmente, en cada caso tener uno o más átomos de hidrogeno reemplazados por halogeno, -OH, alquilo C1-3, -OCO-alquilo C1-3 o cicloalquilo C3-13; con la salvedad de que cuando R4 representa la porcion A en donde R6 representa cicloalquilo C3-13 opcionalmente conteniendo uno o más heteroátomos incorporados en el mismo, el heteroátomo no es nitrogeno; P y Q se seleccionan independientemente de hidrogeno y alquilo C1-3, o P y Q pueden unirse con el átomo de carbono al cual se encuentran anexos para formar cicloalquilo C3-8 como se representa en la porcion (A-1) en donde m1 es 1 y n2 es 0,1, 2, 3, 4 o 5 y R6 es un arilo como se define precedentemente; o P y R6 pueden unirse para formar un sistema cíclico como lo representa la porcion (A-2), en donde m1 es 1 y n2 es 0, 1, 2 3 o 4 y el anillo G es un arilo como se define precedentemente; X representa una union doble o triple; J, K y L se seleccionan independientemente del un grupo que consiste de hidrogeno, halogeno, alquilo C1-10, cicloalquilo C3-13, -OH, -O-alquilo C1-10, O-cicloalquilo C3-13, -OCO-alquilo C1-10, -OCO-cicloalquilo C3-13, -OCO-CO-O-alquilo C1-10, -OCO-CO-O-icloalquilo C3-13, - OCO-O-alquilo C1-10, -OCO-O-cicloalquilo C3-13, -OCO-NH-alquilo C1-10, -OCO-NH-cicloalquilo C3-13, -OCO-N-[(alquilo C1-10)]2, -OCO-N-[(cicloalquilo C3-13)]2, -OCO-NHSO2-alquilo C1-10, - OCO- NHSO2-cicloalquilo C3-13, -NH2, -NH-alquilo C1-8, -N- [(alquilo C1-18)]2, -NO2 y -CN; en donde los grupos alquilo o cicloalquilo pueden contener opcionalmente una o más no saturaciones y/o pueden tener uno o más heteroátomos incorporados en el mismo y opcionalmente, en cada caso tener uno o más átomos de hidrogeno reemplazados por halogeno, -OH, alquilo C1-3, -O-alquilo C1-3, -OCO-alquilo C1-3, -COOH, -COO-alquilo C1-5, -COO-haloalquilo C1-5, -NHCO-alquilo C1-8, -ONO2, -NH-alquilo C1-8, -N-[(alquilo C1-8)]2, -NO2, -CN, cicloalquilo C3-13, arilo o radical heterocíclico; o J y K pueden unirse con el átomo de carbono al cual se anexan para representar un grupo cicloalquilo C3-13 o -CO- y L es lo definido precedentemente; o J, K y L están ausentes cuando n1 es 0; R7 representa un grupo seleccionado de hidrogeno, halogeno, arilo y CO-arilo, en donde el anillo o sistema de anillo se encuentra no sustituido o sustituido como se define precedentemente; o R7, representa la porcion (C-1), en donde n1, J, K y L son lo definido precedentemente, X representa una union simple, doble o triple, m2 es 0, 1 o 2 y m3 es 0, 1 o 2.
ARP070100355A 2006-01-27 2007-01-26 11b-hidroxiandrosta-4-eno-3-onas AR059216A1 (es)

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US (1) US8785425B2 (es)
EP (1) EP2004667B1 (es)
JP (1) JP5097129B2 (es)
KR (1) KR101390272B1 (es)
CN (1) CN101384610B (es)
AP (1) AP2642A (es)
AR (1) AR059216A1 (es)
AU (1) AU2007220114B2 (es)
BR (1) BRPI0706767A2 (es)
CA (1) CA2637548C (es)
EA (1) EA017490B9 (es)
EC (1) ECSP088689A (es)
ES (1) ES2428066T3 (es)
IL (1) IL192983A (es)
MX (1) MX2008009173A (es)
NZ (1) NZ569867A (es)
SG (1) SG170049A1 (es)
TW (1) TWI374147B (es)
UA (1) UA95095C2 (es)
WO (1) WO2007099548A2 (es)
ZA (1) ZA200806366B (es)

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CN111662353A (zh) * 2019-03-05 2020-09-15 上海谷森医药有限公司 一种糠酸氟替卡松晶型1的制备方法

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AR059216A1 (es) 2006-01-27 2008-03-19 Sun Pharmaceutical Ind Ltd 11b-hidroxiandrosta-4-eno-3-onas

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BRPI0706767A2 (pt) 2011-06-28
KR101390272B1 (ko) 2014-05-19
KR20080091813A (ko) 2008-10-14
AP2642A (en) 2013-04-15
CA2637548A1 (en) 2007-09-07
WO2007099548A2 (en) 2007-09-07
NZ569867A (en) 2011-06-30
UA95095C2 (en) 2011-07-11
WO2007099548A3 (en) 2008-10-09
AP2008004558A0 (en) 2008-08-31
CA2637548C (en) 2014-09-23
ES2428066T3 (es) 2013-11-05
ECSP088689A (es) 2008-11-27
SG170049A1 (en) 2011-04-29
EA017490B1 (ru) 2012-12-28
EA200801596A1 (ru) 2009-04-28
IL192983A (en) 2014-06-30
EP2004667A2 (en) 2008-12-24
JP5097129B2 (ja) 2012-12-12
TW200804407A (en) 2008-01-16
US20090054388A1 (en) 2009-02-26
MX2008009173A (es) 2009-01-15
JP2009524649A (ja) 2009-07-02
AU2007220114B2 (en) 2011-11-10
EP2004667B1 (en) 2013-09-04
EA017490B9 (ru) 2013-04-30
EP2004667A4 (en) 2012-07-18
TWI374147B (en) 2012-10-11
US8785425B2 (en) 2014-07-22
IL192983A0 (en) 2009-02-11
CN101384610A (zh) 2009-03-11
CN101384610B (zh) 2013-07-17
AU2007220114A1 (en) 2007-09-07
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