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

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C311/00—Amides 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
    • C07C311/15—Sulfonamides having sulfur atoms of sulfonamide groups bound to carbon atoms of six-membered aromatic rings
    • C07C311/16—Sulfonamides 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
    • C07C311/17—Sulfonamides 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
    • 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
    • A61K31/435—Heterocyclic 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
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/4439—Non 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/18—Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/22—Anxiolytics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/24—Antidepressants
    • 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
    • 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
    • A61P5/44—Glucocorticosteroids; Drugs increasing or potentiating 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
    • A61P5/38—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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C311/00—Amides 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
    • C07C311/22—Sulfonamides, the carbon skeleton of the acid part being further substituted by singly-bound oxygen atoms
    • C07C311/29—Sulfonamides, 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D213/00—Heterocyclic 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
    • C07D213/02—Heterocyclic 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
    • C07D213/04—Heterocyclic 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
    • C07D213/60—Heterocyclic 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
    • C07D213/61—Halogen atoms or nitro radicals
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D213/00—Heterocyclic 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
    • C07D213/02—Heterocyclic 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
    • C07D213/04—Heterocyclic 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
    • C07D213/60—Heterocyclic 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
    • C07D213/78—Carbon atoms having three bonds to hetero atoms, with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C07D213/84—Nitriles
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D261/00—Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings
    • C07D261/02—Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings not condensed with other rings
    • C07D261/06—Heterocyclic 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
    • C07D261/10—Heterocyclic 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D307/00—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom
    • C07D307/02—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom not condensed with other rings
    • C07D307/34—Heterocyclic 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
    • C07D307/56—Heterocyclic 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
    • C07D307/64—Sulfur atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D333/00—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom
    • C07D333/02—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings
    • C07D333/04—Heterocyclic 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
    • C07D333/26—Heterocyclic 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
    • C07D333/30—Hetero atoms other than halogen
    • C07D333/34—Sulfur atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic 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
    • C07D401/02—Heterocyclic 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
    • C07D401/12—Heterocyclic 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

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 (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EA020624B1 (ru) * 2007-07-30 2014-12-30 Арди Байосайенсиз, Инк. Кристаллическая полиморфная форма n-(-)-(3,4-дифтор-2-(2-фтор-4-йодфениламино)-6-метоксифенил)-l-(2,3-дигидроксипропил)циклопропан-1-сульфонамида и ее применение в качестве ингибитора mek
JP2011513409A (ja) * 2008-03-06 2011-04-28 メルク・シャープ・エンド・ドーム・コーポレイション 選択的グルココルチコイドレセプターモジュレーターとしてのヘキサヒドロシクロペンチル［ｆ］インダゾールスルホンアミドおよびこれらの誘導体
ES2579311T3 (es) * 2010-01-15 2016-08-09 Rigel Pharmaceuticals, Inc. Ensayo de exploración empleando DEX y GDF8
US20130190356A1 (en) * 2011-12-22 2013-07-25 Genentech, Inc. Benzyl sulfonamide derivatives as rorc modulators
WO2018005801A2 (en) * 2016-07-01 2018-01-04 Venenum Biodesign Llc Novel non-systemic tgr5 agonists
AR117951A1 (es) * 2018-07-20 2021-09-08 Gruenenthal Gmbh Derivados de triazolquinoxalina adicionalmente sustituidos

Family Cites Families (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1996036595A1 (en) * 1995-05-19 1996-11-21 Chiroscience Limited 3,4-disubstituted-phenylsulphonamides and their therapeutic use
DE60333371D1 (de) 2002-08-29 2010-08-26 Boehringer Ingelheim Pharma 3-(sulfonamidoethyl)-indol-derivate zur verwendung als glucocorticoid-mimetika bei der behandlung von entzündlichen, allergischen und proliferativen erkrankungen
JP2008503490A (ja) * 2004-06-17 2008-02-07 センジェント・セラピューティクス・インコーポレイテッド チロシンホスファターゼの三置換窒素調節物質
SE0402635D0 (sv) * 2004-10-29 2004-10-29 Astrazeneca Ab Chemical compounds

Also Published As

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

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