AR088378A1 - DERIVADOS DE N-CICLOPROPIL-N-(4,5,6,7-TETRAHIDRO-1H-INDAZOL-5-IL)-BENZAMIDA COMO INHIBIDOR DE LA 11b-HSD1 - Google Patents

DERIVADOS DE N-CICLOPROPIL-N-(4,5,6,7-TETRAHIDRO-1H-INDAZOL-5-IL)-BENZAMIDA COMO INHIBIDOR DE LA 11b-HSD1

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Publication number
AR088378A1
AR088378A1 ARP120103883A ARP120103883A AR088378A1 AR 088378 A1 AR088378 A1 AR 088378A1 AR P120103883 A ARP120103883 A AR P120103883A AR P120103883 A ARP120103883 A AR P120103883A AR 088378 A1 AR088378 A1 AR 088378A1
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AR
Argentina
Prior art keywords
substituted
ring
heteroaryl
lower alkyl
pain
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ARP120103883A
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English (en)
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Astellas Pharma Inc
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Publication of AR088378A1 publication Critical patent/AR088378A1/es

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    • C07D231/54Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings condensed with carbocyclic rings or ring systems
    • C07D231/56Benzopyrazoles; Hydrogenated benzopyrazoles
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    • C07D237/00Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings
    • C07D237/26Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings condensed with carbocyclic rings or ring systems
    • C07D237/28Cinnolines
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • A61P25/24Antidepressants
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    • 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
    • A61P27/06Antiglaucoma agents or miotics
    • 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
    • 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
    • A61P3/06Antihyperlipidemics
    • 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
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D239/00Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/70Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings condensed with carbocyclic rings or ring systems
    • C07D239/72Quinazolines; Hydrogenated quinazolines
    • C07D239/78Quinazolines; Hydrogenated quinazolines with hetero atoms directly attached in position 2
    • C07D239/80Oxygen atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
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    • C07D401/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/12Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
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    • C07D471/02Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04Ortho-condensed systems

Abstract

Dar a conocer un compuesto ventajoso como ingrediente activo de una composición farmacéutica para el tratamiento de enfermedades relacionadas con la 11b-hidroxiesteroide deshidrogenasa tipo 1 tales como demencia, esquizofrenia, depresión, dolor (en particular, dolor neuropático o fibromialgia), diabetes (en particular, diabetes mellitus tipo II), la resistencia a la insulina y demás. Se descubrió que un compuesto heterocíclico bicíclico (el heterociclo bicíclico se forma cuando un anillo de ciclohexano se fusiona a un heterociclo monocíclico de 5 a 6 miembros que tiene sólo un átomo de nitrógeno como heteroátomo) sustituido con un grupo acilamino tal como un grupo (hetero)aroilamino similar o una sal farmacéuticamente aceptable del mismo tiene una excelente acción de inhibición contra la 11b-HSD1. En consecuencia, este compuesto heterocíclico bicíclico se puede utilizar para el tratamiento de la demencia, esquizofrenia, depresión, dolor (en particular, dolor neuropático o fibromialgia), diabetes (en particular, diabetes mellitus tipo II), la resistencia a la insulina y demás. Reivindicación 1: Un compuesto representado por la fórmula (1) o una sal farmacéuticamente aceptable del mismo, [los símbolos que aparecen en la fórmula representan lo siguiente: anillo A: un heterociclo monocíclico de 5 a 6 miembros que puede estar sustituido y tiene sólo el o los átomos de nitrógeno como heteroátomos; donde los átomos presentes en la posición en que el anillo se fusiona al anillo adyacente son átomos de carbono, R¹: alquilo inferior, halógeno-alquilo inferior, o cicloalquilo que puede estar sustituido, R²: halógeno o alquilo inferior, R³: arilo, heteroarilo o alquileno inferior-heteroarilo; donde cada uno del arilo y heteroarilo representados por R³ puede estar sustituido, n: un entero de 0 a 3 y una línea de puntos representa un enlace simple o un enlace doble].
ARP120103883A 2011-10-18 2012-10-18 DERIVADOS DE N-CICLOPROPIL-N-(4,5,6,7-TETRAHIDRO-1H-INDAZOL-5-IL)-BENZAMIDA COMO INHIBIDOR DE LA 11b-HSD1 AR088378A1 (es)

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JP2011228822 2011-10-18

Publications (1)

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AR088378A1 true AR088378A1 (es) 2014-05-28

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ARP120103883A AR088378A1 (es) 2011-10-18 2012-10-18 DERIVADOS DE N-CICLOPROPIL-N-(4,5,6,7-TETRAHIDRO-1H-INDAZOL-5-IL)-BENZAMIDA COMO INHIBIDOR DE LA 11b-HSD1

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US (1) US9266840B2 (es)
EP (1) EP2772484B1 (es)
JP (1) JP6020459B2 (es)
KR (1) KR101987514B1 (es)
CN (1) CN103917524B (es)
AR (1) AR088378A1 (es)
AU (1) AU2012327076B2 (es)
BR (1) BR112014009524A2 (es)
CA (1) CA2851589C (es)
CY (1) CY1119181T1 (es)
DK (1) DK2772484T3 (es)
EA (1) EA024846B1 (es)
ES (1) ES2641258T3 (es)
HR (1) HRP20171125T1 (es)
IL (1) IL232061A (es)
IN (1) IN2014CN02949A (es)
LT (1) LT2772484T (es)
ME (1) ME02733B (es)
MX (1) MX344014B (es)
PL (1) PL2772484T3 (es)
PT (1) PT2772484T (es)
RS (1) RS56288B1 (es)
SI (1) SI2772484T1 (es)
TW (1) TWI545113B (es)
UA (1) UA112327C2 (es)
WO (1) WO2013058258A1 (es)
ZA (1) ZA201403513B (es)

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EP2844259A4 (en) 2012-04-30 2015-11-11 Anderson Gaweco MMR MODULATORS AND USES THEREOF
US9045477B2 (en) 2013-03-15 2015-06-02 Epizyme, Inc. Substituted 6,5-fused bicyclic heteroaryl compounds
EP2970306A4 (en) * 2013-03-15 2016-08-03 Epizyme Inc SUBSTITUTED BICYCLIC HETEROARYL COMPOUNDS CONDENSED IN 6.5
AU2016284398C1 (en) * 2015-06-22 2021-01-07 Sumitomo Dainippon Pharma Co., Ltd. 1,4-disubstituted imidazole derivative
CN108129430A (zh) * 2016-11-30 2018-06-08 重庆圣华曦药业股份有限公司 一种立他司特中间体的合成方法
CN115925692A (zh) * 2022-11-28 2023-04-07 浙江理工大学 一种三氟甲基取代的烯胺化合物的制备方法

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EP2772484B1 (en) 2017-06-28
US9266840B2 (en) 2016-02-23
MX344014B (es) 2016-12-02
UA112327C2 (uk) 2016-08-25
IL232061A0 (en) 2014-05-28
CA2851589A1 (en) 2013-04-25
BR112014009524A2 (pt) 2017-05-09
KR101987514B1 (ko) 2019-06-10
ES2641258T3 (es) 2017-11-08
EA201490811A1 (ru) 2014-09-30
EP2772484A1 (en) 2014-09-03
PL2772484T3 (pl) 2017-10-31
AU2012327076A1 (en) 2014-05-01
PT2772484T (pt) 2017-08-04
KR20140081860A (ko) 2014-07-01
IN2014CN02949A (es) 2015-07-03
JP6020459B2 (ja) 2016-11-02
RS56288B1 (sr) 2017-12-29
CN103917524B (zh) 2016-05-04
SI2772484T1 (sl) 2017-11-30
CA2851589C (en) 2019-02-19
EA024846B1 (ru) 2016-10-31
JPWO2013058258A1 (ja) 2015-04-02
HRP20171125T1 (hr) 2017-10-06
ME02733B (me) 2017-10-20
TW201331185A (zh) 2013-08-01
CN103917524A (zh) 2014-07-09
EP2772484A4 (en) 2015-03-25
DK2772484T3 (en) 2017-08-21
US20140249151A1 (en) 2014-09-04
TWI545113B (zh) 2016-08-11
ZA201403513B (en) 2015-11-25
WO2013058258A1 (ja) 2013-04-25
IL232061A (en) 2016-04-21
CY1119181T1 (el) 2018-03-07
AU2012327076B2 (en) 2017-07-06
MX2014004701A (es) 2014-10-14
LT2772484T (lt) 2017-12-27

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