ECSP088602A - Compuestos con efectos medicinales debido a la interacción con el receptor de glucocorticoides - Google Patents

Compuestos con efectos medicinales debido a la interacción con el receptor de glucocorticoides

Info

Publication number
ECSP088602A
ECSP088602A EC2008008602A ECSP088602A ECSP088602A EC SP088602 A ECSP088602 A EC SP088602A EC 2008008602 A EC2008008602 A EC 2008008602A EC SP088602 A ECSP088602 A EC SP088602A EC SP088602 A ECSP088602 A EC SP088602A
Authority
EC
Ecuador
Prior art keywords
optionally halogenated
alkoxy
alkyl
hydrogen
halogen
Prior art date
Application number
EC2008008602A
Other languages
English (en)
Inventor
Koc-Kan Ho
Michael Ohlmeyer
John Richard Morphy
Niall Morton Hamilton
Simon James Anthony Grove
Michael John Kiczun
Brad Sherborne
Peter Thomas Albert Littlewood
Angus Richard Brown
Celia Kingsbury
Steven G Kultgen
Original Assignee
Organon Nv
Pharmacopeia 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 Organon Nv, Pharmacopeia Inc filed Critical Organon Nv
Publication of ECSP088602A publication Critical patent/ECSP088602A/es

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Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C311/00Amides of sulfonic acids, i.e. compounds having singly-bound oxygen atoms of sulfo groups replaced by nitrogen atoms, not being part of nitro or nitroso groups
    • C07C311/15Sulfonamides having sulfur atoms of sulfonamide groups bound to carbon atoms of six-membered aromatic rings
    • C07C311/16Sulfonamides having sulfur atoms of sulfonamide groups bound to carbon atoms of six-membered aromatic rings having the nitrogen atom of at least one of the sulfonamide groups bound to hydrogen atoms or to an acyclic carbon atom
    • C07C311/17Sulfonamides having sulfur atoms of sulfonamide groups bound to carbon atoms of six-membered aromatic rings having the nitrogen atom of at least one of the sulfonamide groups bound to hydrogen atoms or to an acyclic carbon atom to an acyclic carbon atom of a hydrocarbon radical substituted by singly-bound oxygen atoms
    • 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
    • A61K31/435Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/4439Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
    • 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
    • A61P25/22Anxiolytics
    • 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
    • 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
    • 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
    • A61P5/44Glucocorticosteroids; Drugs increasing or potentiating 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
    • A61P5/38Drugs 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C311/00Amides of sulfonic acids, i.e. compounds having singly-bound oxygen atoms of sulfo groups replaced by nitrogen atoms, not being part of nitro or nitroso groups
    • C07C311/22Sulfonamides, the carbon skeleton of the acid part being further substituted by singly-bound oxygen atoms
    • C07C311/29Sulfonamides, the carbon skeleton of the acid part being further substituted by singly-bound oxygen atoms having the sulfur atom of at least one of the sulfonamide groups bound to a carbon atom of a six-membered aromatic ring
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D213/00Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/60Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom 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
    • C07D213/61Halogen atoms or nitro radicals
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D213/00Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/60Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom 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
    • C07D213/78Carbon atoms having three bonds to hetero atoms, with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C07D213/84Nitriles
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D261/00Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings
    • C07D261/02Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings not condensed with other rings
    • C07D261/06Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings not condensed with other rings having two or more double bonds between ring members or between ring members and non-ring members
    • C07D261/10Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings not condensed with other rings having two or more 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
    • C07D307/00Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom
    • C07D307/02Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom not condensed with other rings
    • C07D307/34Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D307/56Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom 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
    • C07D307/64Sulfur atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D333/00Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom
    • C07D333/02Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings
    • C07D333/04Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings not substituted on the ring sulphur atom
    • C07D333/26Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings not substituted on the ring sulphur atom 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
    • C07D333/30Hetero atoms other than halogen
    • C07D333/34Sulfur atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • 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

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Neurosurgery (AREA)
  • Endocrinology (AREA)
  • Diabetes (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Psychiatry (AREA)
  • Pain & Pain Management (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Pyridine Compounds (AREA)

Abstract

La invención provee compuestos que tienen la estructura de acuerdo con la fórmula I, en donde: X es un átomo de carbono o de nitrógeno; Ar es fenilo o un anillo heteroaromático; R1 es hidrógeno, halógeno, CN o alquilo(C1-C4); R2 es hidrógeno, halógeno o alcoxi(C1-C3) opcionalmente fluorinado; R3 y R5 son independientemente hidrógeno, alquilo(C1-C4) opcionalmente halogenado, alcoxi (C1-C4) opcionalmente halogenado, arilalcoxi(C1-C4) opcionalmente halogenado, alquenilo(C1-C4) opcionalmente halogenado o hidroxilmetilo; R4 es hidrógeno, halógeno, alcoxi(C1-C4) opcionalmente halogenado o arilalcoxi(C1-C4) opcionalmente halogenado; R6 es hidrógeno, bencilo, opcionalmente sustituido con uno o más halógenos o alquilo(C1-C4), o R6 es alquilo(C1-C4) opcionalmente halogenado; cada R7 es independientemente hidrógeno, halógeno, alquilo(C1-C4) opcionalmente halogenado o alcoxi(C1-C4) opcionalmente halogenado y sales de adición ácida farmacéuticamente adecuadas de los mismos, para uso como moduladores del receptor de glucocorticoides, en particular para el tratamiento de trastornos del sistema nervioso central.
EC2008008602A 2005-12-21 2008-07-04 Compuestos con efectos medicinales debido a la interacción con el receptor de glucocorticoides ECSP088602A (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US75252605P 2005-12-21 2005-12-21

Publications (1)

Publication Number Publication Date
ECSP088602A true ECSP088602A (es) 2008-08-29

Family

ID=37902853

Family Applications (1)

Application Number Title Priority Date Filing Date
EC2008008602A ECSP088602A (es) 2005-12-21 2008-07-04 Compuestos con efectos medicinales debido a la interacción con el receptor de glucocorticoides

Country Status (19)

Country Link
US (1) US7960365B2 (es)
EP (1) EP1965785A1 (es)
JP (1) JP5319299B2 (es)
KR (1) KR20080086482A (es)
CN (1) CN101534811A (es)
AR (1) AR058576A1 (es)
AU (1) AU2006328550B2 (es)
BR (1) BRPI0620184A2 (es)
CA (1) CA2631816C (es)
EC (1) ECSP088602A (es)
IL (1) IL191815A0 (es)
MX (1) MX2008007681A (es)
NO (1) NO20082436L (es)
NZ (1) NZ569011A (es)
PE (1) PE20071170A1 (es)
RU (1) RU2430086C2 (es)
TW (1) TW200800150A (es)
WO (1) WO2007071638A1 (es)
ZA (1) ZA200804643B (es)

Families Citing this family (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2010535232A (ja) * 2007-07-30 2010-11-18 アルディア バイオサイエンス,インク. Mekの阻害剤としての多形体を含む、n−(アリールアミノ)スルホンアミドの誘導体、および組成物、使用方法、ならびにその調製方法
CA2716136A1 (en) * 2008-03-06 2009-09-11 William P. Dankulich Hexahydrocyclopentyl[f]indazole sulfonamides and derivatives thereof as selective glucocorticoid receptor modulators
CA2786086A1 (en) * 2010-01-15 2011-07-21 Rigel Pharmaceuticals, Inc. Screening assay employing dex and gdf8
US20130190356A1 (en) * 2011-12-22 2013-07-25 Genentech, Inc. Benzyl sulfonamide derivatives as rorc modulators
US11236055B2 (en) 2016-07-01 2022-02-01 Venenum Biodesign, LLC Non-systemic TGR5 agonists
KR102741244B1 (ko) * 2017-12-19 2024-12-11 인터내셔널 엔&에이치 덴마크 에이피에스 인지 및 정신 건강을 위한 프로바이오틱스
US10981918B2 (en) * 2018-07-20 2021-04-20 Grünenthal GmbH Further substituted triazolo quinoxaline derivatives

Family Cites Families (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
NZ247440A (en) * 1992-05-06 1995-04-27 Squibb & Sons Inc Phenyl sulphonamide derivatives, preparation and pharmaceutical compositions thereof
WO1996036595A1 (en) * 1995-05-19 1996-11-21 Chiroscience Limited 3,4-disubstituted-phenylsulphonamides and their therapeutic use
GB9702194D0 (en) * 1997-02-04 1997-03-26 Lilly Co Eli Sulphonide derivatives
EP1539141B1 (en) * 2002-08-29 2010-07-14 Boehringer Ingelheim Pharmaceuticals Inc. 3-(sulfonamidoethyl)-indole derivatives for use as glucocorticoid mimetics in the treatment of inflammatory, allergic and proliferative diseases
US20060135773A1 (en) * 2004-06-17 2006-06-22 Semple Joseph E Trisubstituted nitrogen modulators of tyrosine phosphatases
SE0402635D0 (sv) * 2004-10-29 2004-10-29 Astrazeneca Ab Chemical compounds

Also Published As

Publication number Publication date
JP5319299B2 (ja) 2013-10-16
RU2430086C2 (ru) 2011-09-27
CN101534811A (zh) 2009-09-16
JP2009526749A (ja) 2009-07-23
US20070149577A1 (en) 2007-06-28
IL191815A0 (en) 2008-12-29
RU2008129667A (ru) 2010-01-27
WO2007071638A1 (en) 2007-06-28
US7960365B2 (en) 2011-06-14
CA2631816C (en) 2014-05-06
TW200800150A (en) 2008-01-01
PE20071170A1 (es) 2007-11-30
AU2006328550B2 (en) 2012-04-12
AR058576A1 (es) 2008-02-13
BRPI0620184A2 (pt) 2011-11-01
KR20080086482A (ko) 2008-09-25
CA2631816A1 (en) 2007-06-28
AU2006328550A1 (en) 2007-06-28
ZA200804643B (en) 2009-03-25
MX2008007681A (es) 2008-10-23
EP1965785A1 (en) 2008-09-10
NZ569011A (en) 2011-04-29
NO20082436L (no) 2008-09-08

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