PE20120355A1 - DERIVADOS DE PIRAZOL COMO INHIBIDORES DE LA ENZIMA 11ßHSD1 - Google Patents

DERIVADOS DE PIRAZOL COMO INHIBIDORES DE LA ENZIMA 11ßHSD1

Info

Publication number
PE20120355A1
PE20120355A1 PE2012000020A PE2012000020A PE20120355A1 PE 20120355 A1 PE20120355 A1 PE 20120355A1 PE 2012000020 A PE2012000020 A PE 2012000020A PE 2012000020 A PE2012000020 A PE 2012000020A PE 20120355 A1 PE20120355 A1 PE 20120355A1
Authority
PE
Peru
Prior art keywords
alkyl
11ßhsd1
propylsulfanil
cycloalkanylidene
pirazol
Prior art date
Application number
PE2012000020A
Other languages
English (en)
Inventor
Paul Robert Owen Whittamore
James Stewart Scott
Martin John Packer
Andrew Stocker
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=***_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=PE20120355(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 PE20120355A1 publication Critical patent/PE20120355A1/es

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D231/00Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
    • C07D231/02Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings
    • C07D231/10Heterocyclic 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
    • C07D231/14Heterocyclic 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
    • C07D231/18One oxygen or sulfur atom
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41Heterocyclic 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
    • A61K31/4151,2-Diazoles
    • 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
    • A61P3/08Drugs 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00Drugs for disorders of the endocrine system
    • A61P5/38Drugs for disorders of the endocrine system of the suprarenal hormones
    • A61P5/46Drugs for disorders of the endocrine system of the suprarenal hormones for decreasing, blocking or antagonising the activity of glucocorticosteroids
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00Drugs for disorders of the endocrine system
    • A61P5/48Drugs for disorders of the endocrine system of the pancreatic hormones
    • A61P5/50Drugs for disorders of the endocrine system of the pancreatic hormones for increasing or potentiating the activity of insulin
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/12Antihypertensives
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D231/00Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
    • C07D231/02Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings
    • C07D231/10Heterocyclic 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
    • C07D231/14Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02Heterocyclic 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
    • C07D403/06Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D405/00Heterocyclic 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
    • C07D405/02Heterocyclic 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
    • C07D405/12Heterocyclic 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

Abstract

REFERIDA A UN COMPUESTO DERIVADO DE PIRAZOL DE FORMULA (1), DONDE Q ES O, S O UN ENLACE SIMPLE; R1 ES ALQUILO C1-C6, ALQUENILO C2-C6, ALQUINILO C2-C6, ENTRE OTROS; R2 ES CICLOALQUIL C3-C7(CH2)m, POLICICLOALQUILC6-C12(CH2)m, ENTRE OTROS; R3 ES H, ALQUILO C1-C4-CICLALQUILO C3-C5, CICLOALQUILMETILO C3-C5, ENTRE OTROS; A ES UN ANILLO FENILO O HETEROARILO OPCIONALMENTE SUSTITUIDOS CON R10 O R11; R10 ES ALQUILO C1-C4, OH, CIANO, TRIFLUOROMETILO, HALO, ENTRE OTROS; R11 ES ALQUILO C1-C3 OPCIONALMENTE SUSTITUIDO CON FLUOR; X ES UN ENLACE DIRECTO, CICLOALCANDIILO C3-C4, CICLOALCANILIDENO C3-C4, CH2O, ENTRE OTROS; Y ES UN ENLACE DIRECTO, CICLOALCANDIILO C3-C4, CICLOALCANILIDENO C3-C4, ENTRE OTROS; m ES 0 A 2. SON COMPUESTOS PREFERIDOS: ACIDO 4-[4-[[(1S,3R)-5-HIDROXI-2-ADAMANTIL]CARBAMOIL]-5-PROPILSULFANIL-PIRAZOL-1-IL]BENZOICO, ACIDO 4-[4-(2-ADAMANTILCARBAMOIL)-5-PROPILSULFANIL-PIRAZOL-1-IL]BENZOICO, ACIDO 4-[4-(OXAN-4-ILCARBAMOIL)-5-PROPILSULFANIL-PIRAZOL-1-IL]BENZOICO, ENTRE OTROS. REFERIDA A UNA COMPOSICION FARMACEUTICA Y A UN PROCESO DE PREPARACION. DICHOS COMPUESTOS SON INHIBIDORES DE LA ENZIMA 11-BETA-HIDROXIESTEROIDE DESHIDROGENASA DE TIPO 1 HUMANA (11ßHSD1) Y SON UTILES EN EL TRATAMIENTO DE ENFERMEDADES RELACIONADAS CON EL SINDROME METABOLICO
PE2012000020A 2007-02-12 2008-02-11 DERIVADOS DE PIRAZOL COMO INHIBIDORES DE LA ENZIMA 11ßHSD1 PE20120355A1 (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
PE20120355A1 true PE20120355A1 (es) 2012-05-17

Family

ID=39438215

Family Applications (2)

Application Number Title Priority Date Filing Date
PE2008000295A PE20090649A1 (es) 2007-02-12 2008-02-11 DERIVADOS DE PIRAZOL COMO INHIBIDORES DE LA ENZIMA 11ßHSD1
PE2012000020A PE20120355A1 (es) 2007-02-12 2008-02-11 DERIVADOS DE PIRAZOL COMO INHIBIDORES DE LA ENZIMA 11ßHSD1

Family Applications Before (1)

Application Number Title Priority Date Filing Date
PE2008000295A PE20090649A1 (es) 2007-02-12 2008-02-11 DERIVADOS DE PIRAZOL COMO INHIBIDORES DE LA ENZIMA 11ßHSD1

Country Status (23)

Country Link
US (2) US7816391B2 (es)
EP (2) EP2292228A1 (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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Also Published As

Publication number Publication date
ZA201000838B (en) 2010-10-27
JP2010518063A (ja) 2010-05-27
IL200047A0 (en) 2010-04-15
RU2012125372A (ru) 2013-12-27
AU2008215976B2 (en) 2011-11-24
WO2008099145A1 (en) 2008-08-21
UY30912A1 (es) 2008-09-30
CN102503891A (zh) 2012-06-20
EP2292228A1 (en) 2011-03-09
SG177892A1 (en) 2012-02-28
CO6220949A2 (es) 2010-11-19
AR065300A1 (es) 2009-05-27
RU2462456C2 (ru) 2012-09-27
EP2124937A1 (en) 2009-12-02
US8344016B2 (en) 2013-01-01
PE20090649A1 (es) 2009-06-26
MX2009008506A (es) 2009-10-12
NZ578568A (en) 2012-01-12
US7816391B2 (en) 2010-10-19
BRPI0808450A2 (pt) 2014-08-12
CL2008000422A1 (es) 2009-01-02
US20110224273A1 (en) 2011-09-15
TW200836719A (en) 2008-09-16
RU2009133259A (ru) 2011-03-20
AU2008215976A1 (en) 2008-08-21
CA2676154A1 (en) 2008-08-21
SA08290055B1 (ar) 2012-09-26
ECSP099571A (es) 2009-09-29
US20090221663A1 (en) 2009-09-03
KR20090108726A (ko) 2009-10-16

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