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AR065300A1 - Compuestos quimicos derivados de 1,2-pirazol - Google Patents

Compuestos quimicos derivados de 1,2-pirazol

Info

Publication number
AR065300A1
AR065300A1 ARP080100584A ARP080100584A AR065300A1 AR 065300 A1 AR065300 A1 AR 065300A1 AR P080100584 A ARP080100584 A AR P080100584A AR P080100584 A ARP080100584 A AR P080100584A AR 065300 A1 AR065300 A1 AR 065300A1
Authority
AR
Argentina
Prior art keywords
alkyl
optionally substituted
independently selected
cyano
halo
Prior art date
Application number
ARP080100584A
Other languages
English (en)
Original Assignee
Astrazeneca Ab
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
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=39438215&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=AR065300(A1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Astrazeneca Ab filed Critical Astrazeneca Ab
Publication of AR065300A1 publication Critical patent/AR065300A1/es

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D231/00—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
    • C07D231/02—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings
    • C07D231/10—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D231/14—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D231/18—One oxygen or sulfur atom
    • 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
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/415—1,2-Diazoles
    • 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
    • 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
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • 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
    • A61P5/38—Drugs for disorders of the endocrine system of the suprarenal hormones
    • A61P5/46—Drugs for disorders of the endocrine system of the suprarenal hormones for decreasing, blocking or antagonising the activity of glucocorticosteroids
    • 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
    • A61P5/48—Drugs for disorders of the endocrine system of the pancreatic hormones
    • A61P5/50—Drugs for disorders of the endocrine system of the pancreatic hormones for increasing or potentiating the activity of insulin
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/12—Antihypertensives
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D231/00—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
    • C07D231/02—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings
    • C07D231/10—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D231/14—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/06—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
    • C07D405/12—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Diabetes (AREA)
  • Medicinal Chemistry (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Endocrinology (AREA)
  • Obesity (AREA)
  • Hematology (AREA)
  • Child & Adolescent Psychology (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Emergency Medicine (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)

Abstract

Compuestos utiles en la inhibicion de 11betaHSD1; procesos para su elaboracion y composiciones farmacéuticas que los comprenden. Reivindicacion 1: Un compuesto de la formula (1): donde: Q es O, S o un enlace simple; R1 es alquilo C1-6, alquenilo C2- 6, alquinilo C2-6, cicloalquilo C3-7, heterociclilo, aril-alquiIoC1-3, heteroariI-alquiloC1-3, cicloalquilC3-7-alquiloC1-3, cicloalquilC3-7-alqueniloC2-3 o cicloalquilC3-7-alquiniloC2-3 [donde cada sin esta opcionalmente sustituido con 1, 2 o 3 sustituyentes seleccionados de manera independiente de alquilo C1-3, hidroxi, halo, oxo, ciano, trifluormetilo, alcoxi C1-3, alquiloC1-3S(O)n- (donde n es 0, 1, 2 o 3), R5CON(R5')-, (R5)(R5'')NC(O)-, R5'C(O)O-, R5'OC(O)-, (R5')(R5'')NC(O)N(R5ö')-, R5SO2N(R5'')- y (R5')(R5ö)NSO2- (donde R5 es alquilo C1-3 opcionalmente sustituido con 1, 2 o 3 sustituyentes seleccionados de hidroxilo, halo o ciano; y R5' y R5''se seleccionan de manera independiente de hidrogeno y alquilo C1-3 opcionalmente sustituido con 1, 2 o 3 sustituyentes seleccionados de manera independiente de hidroxilo, halo, alcoxi C1-3, carboxi y ciano; o R5' y R5'' junto con el átomo de nitrogeno al cual están unidos forman un anillo saturado de 4 a 7 miembros )]; R2 se selecciona de heterociclilo, cicloalquiloC3-7(CH2)m-, y policicloalquiloC6-12(CH2)m- (donde m es 0, 1 o 2, y los anillos están opcionalmente sustituidos con 1, 2 o 3 sustituyentes seleccionados de manera independiente de R6); R3 se selecciona de hidrogeno, aIquilo C1-4, cicloalquilo C3-5 y cicloalquilmetilo C3-5 (donde cada uno está opcionalmente sustituido con 1, 2 o 3 átomos de fluor); R2 y R3 junto con el átomo de nitrogeno al cual están unidos forman un sistema de anillo monocíclico, bicíclico o puenteado, saturado, que, en forma opcional, contiene 1 o 2 heteroátomos de anillo adicionales seleccionados de nitrogeno, oxígeno y azufre, y que está opcionalmente fusionado a un anillo monocíclico saturado, parcialmente saturado o insaturado, donde el sistema de anillo resultante está opcionalmente sustituido con 1, 2 o 3 sustituyentes seleccionados de modo independiente de R7; R6 y R7 se seleccionan de manera independiente de hidroxilo, halo, oxo, carboxi, ciano, trifluormetilo, R9, R9O-, R9CO-, R9C(O)O-, R9CON(R9')-, (R9')(R9'')NC(O)-, (R9')(R9ö)N-, R9S(O)a- donde a es 0 a 2, R9'OC(O)-, (R9')(R9ö)NSO2-, R9SO2N(R9)-, (R9')(R9ö)NC(O)N(R9'')-, fenilo y heteroarilo [donde los grupos fenilo y heteroarilo están opcionalmente fusionados a un fenilo, heteroarilo o un anillo de 5 o 6 miembros saturado o parcialmente saturado que, en forma opcional, contiene 1, 2 o 3 heteroátomos seleccionados de manera independiente de nitrogeno, oxígeno y azufre, donde el sistema de anillo resultante está opcionalmente sustituido con 1, 2 o 3 sustituyentes seleccionados de modo independiente de alquilo C1-4, hidroxilo, ciano, trifluormetilo, trifluormetoxi, halo, alcoxi C1-4, alcoxiC1-4-alquiloC1-4, amino, N- alquilaminoC1-4, di-N,N-(alquilo C1-4)amino, N-alquilcarbamoiloC1-4, di-N,N-(alquilo C1-4)carbamoilo, alquilC1-4S(O)r-, alquilC1-4S(O)alquiIoC1-4 (donde r es 0, 1 u 2)]; R9 se selecciona de manera independiente de alquilo C1-3 opcionalmenle sustituido con hidroxilo, hato, alcoxi C1-4, carboxi o ciano; R9', R9ö y R9''' se seleccionan de manera independiente de hidrogeno y alquilo C1-3 opcionalmente sustituido con 1, 2, o 3 sustituyentes seleccionados de manera independiente de hidroxilo, halo, alcoxi C1-4, carboxi y ciano; A es un anillo fenilo o heteroarilo (donde el anillo fenilo o heteroarilo está opcionalmente sustituido en átomos de carbono del anillo, con 1, 2 u 3 grupos R10, y en un nitrogeno de anillo disponible en un grupo heteroarilo, con R11); R10 se selecciona de manera independiente de alquilo C1-4, hidroxilo, ciano, trifluormetilo, trifluormetoxi, halo, alcoxi C1-4, alcoxiC1-4-alquiloC1-4, amino, N-alquilaminoC1-4, di-N,N-(alquilo C1-4)amino, N- alquilcarbamoíloC1-4, di-N,N-(alquilo C1-4)carbamoílo, aIquiloC1-4S(O)s-, alquiloC1-4S(O)salquiloC1-4 (donde s es 0, 1 o 2)]; R11 es, de manera independiente, alquilo C1-3 opcionalmente sustituido con 1, 2 o 3 átomos de fluor; X es un enlace directo, cicloalcanodiílo C3-4, cicloalcanilideno C3-4, -C(R12)(R13)-, -C(R12)(R13)C(R14)(R15)-, -CH2O- o -CH2S(O)t- (donde t es 0, 1 o 2): Y es un enlace directo, cicloalcanodiílo C3-4, cicloalcanilideno C3-4, -C(R16)(R17)- o - C(R18)(R19)C(R20)(R21)-; donde R12, R13, R14, R15, R16, R17, R18, R19, R20 y R21se seleccionan de manera independiente de hidrogeno y metilo; o una de sus sales aceptables para uso farmacéutico.
ARP080100584A 2007-02-12 2008-02-11 Compuestos quimicos derivados de 1,2-pirazol AR065300A1 (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US88933607P 2007-02-12 2007-02-12
US98573507P 2007-11-06 2007-11-06

Publications (1)

Publication Number Publication Date
AR065300A1 true AR065300A1 (es) 2009-05-27

Family

ID=39438215

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP080100584A AR065300A1 (es) 2007-02-12 2008-02-11 Compuestos quimicos derivados de 1,2-pirazol

Country Status (23)

Country Link
US (2) US7816391B2 (es)
EP (2) EP2124937A1 (es)
JP (1) JP2010518063A (es)
KR (1) KR20090108726A (es)
CN (1) CN102503891A (es)
AR (1) AR065300A1 (es)
AU (1) AU2008215976B2 (es)
BR (1) BRPI0808450A2 (es)
CA (1) CA2676154A1 (es)
CL (1) CL2008000422A1 (es)
CO (1) CO6220949A2 (es)
EC (1) ECSP099571A (es)
IL (1) IL200047A0 (es)
MX (1) MX2009008506A (es)
NZ (1) NZ578568A (es)
PE (2) PE20090649A1 (es)
RU (2) RU2462456C2 (es)
SA (1) SA08290055B1 (es)
SG (1) SG177892A1 (es)
TW (1) TW200836719A (es)
UY (1) UY30912A1 (es)
WO (1) WO2008099145A1 (es)
ZA (1) ZA201000838B (es)

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IL200047A0 (en) 2010-04-15
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US20090221663A1 (en) 2009-09-03
RU2009133259A (ru) 2011-03-20
CA2676154A1 (en) 2008-08-21
PE20090649A1 (es) 2009-06-26
BRPI0808450A2 (pt) 2014-08-12
CN102503891A (zh) 2012-06-20
ZA201000838B (en) 2010-10-27
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US8344016B2 (en) 2013-01-01
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