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NO20053596L - Adamantylacetamider som 11-beta hydroksysteroid-dehydrogenaseinhibitorer - Google Patents

Adamantylacetamider som 11-beta hydroksysteroid-dehydrogenaseinhibitorer

Info

Publication number
NO20053596L
NO20053596L NO20053596A NO20053596A NO20053596L NO 20053596 L NO20053596 L NO 20053596L NO 20053596 A NO20053596 A NO 20053596A NO 20053596 A NO20053596 A NO 20053596A NO 20053596 L NO20053596 L NO 20053596L
Authority
NO
Norway
Prior art keywords
alkyl
cycloalkyl
4alkyloxy
het1
substituents
Prior art date
Application number
NO20053596A
Other languages
English (en)
Other versions
NO331456B1 (no
Inventor
Louis Jozef Elisabeth Va Veken
Joannes Theodorus Mari Linders
Gustaaf Henri Maria Willemsens
Ronaldus Arnodus Gilissen
Christophe Francis Rober Buyck
Greta Constantia Peter Vanhoof
Libuse Jsaroskova
Original Assignee
Janssen Pharmaceutica Nv
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 Janssen Pharmaceutica Nv filed Critical Janssen Pharmaceutica Nv
Publication of NO20053596L publication Critical patent/NO20053596L/no
Publication of NO331456B1 publication Critical patent/NO331456B1/no

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    • C07D207/00—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D207/02—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D207/18—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having one double bond between ring members or between a ring member and a non-ring member
    • C07D207/22—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having one double bond between ring members or between a ring member and a non-ring member 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
    • C07D207/24—Oxygen or sulfur atoms
    • C07D207/26—2-Pyrrolidones
    • C07D207/263—2-Pyrrolidones with only hydrogen atoms or radicals containing only hydrogen and carbon atoms directly attached to other ring carbon atoms
    • C07D207/27—2-Pyrrolidones with only hydrogen atoms or radicals containing only hydrogen and carbon atoms directly attached to other ring carbon atoms with substituted hydrocarbon radicals directly attached to the ring nitrogen atom
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    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/16—Amides, e.g. hydroxamic acids
    • A61K31/165—Amides, e.g. hydroxamic acids having aromatic rings, e.g. colchicine, atenolol, progabide
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    • C07C233/11—Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms having nitrogen atoms of carboxamide groups bound to hydrogen atoms or to carbon atoms of unsubstituted hydrocarbon radicals with carbon atoms of carboxamide groups bound to carbon atoms of an unsaturated carbon skeleton containing six-membered aromatic rings
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    • C07C233/23—Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by singly-bound oxygen atoms with the substituted hydrocarbon radical bound to the nitrogen atom of the carboxamide group by a carbon atom of a ring other than a six-membered aromatic ring
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    • C07C233/30—Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by doubly-bound oxygen atoms
    • C07C233/32—Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by doubly-bound oxygen atoms with the substituted hydrocarbon radical bound to the nitrogen atom of the carboxamide group by a carbon atom of a ring other than a six-membered aromatic ring
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    • C07C233/34—Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by amino groups
    • C07C233/41—Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by amino groups with the substituted hydrocarbon radical bound to the nitrogen atom of the carboxamide group by a carbon atom of a ring other than a six-membered aromatic ring
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    • C07C235/32—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms having carbon atoms of carboxamide groups bound to acyclic carbon atoms and singly-bound oxygen atoms bound to the same carbon skeleton the carbon skeleton containing six-membered aromatic rings
    • C07C235/36—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms having carbon atoms of carboxamide groups bound to acyclic carbon atoms and singly-bound oxygen atoms bound to the same carbon skeleton the carbon skeleton containing six-membered aromatic rings having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a ring other than a six-membered aromatic ring
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    • C07C237/20—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups having the carbon atoms of the carboxamide groups bound to acyclic carbon atoms of the carbon skeleton the carbon skeleton containing six-membered aromatic rings
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    • C07C237/22—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups having the carbon atoms of the carboxamide groups bound to acyclic carbon atoms of the carbon skeleton having nitrogen atoms of amino groups bound to the carbon skeleton of the acid part, further acylated
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    • C07C255/41—Carboxylic acid nitriles having cyano groups bound to acyclic carbon atoms having cyano groups bound to acyclic carbon atoms of a carbon skeleton containing at least one six-membered aromatic ring the carbon skeleton being further substituted by carboxyl groups, other than cyano groups
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Abstract

N-oksidformene, de farmasøytisk akseptable addisjonssalter og de stereokjemisk isomere former derav, hvori n representerer et heltall som er 1 eller 2; R1 og R2 representerer hver uavhengig hydrogen C1-4alkyl, NR9R10, C 1-4alkyloksy; eller R1 og R2 tatt sammen med karbonatomet til hvilket de er bundet danner et C3-6sykloalkyl; og der n er 2, kan enten R1 eller R2 være fraværende for å danne en umettet binding; R3 representerer et C6-12sykloalkyl, fortrinnsvis valgt fra syklooktanyl og sykloheksyl eller R3 representerer et monovalent radikal som har én av de følgende formler hvori nevnte C6-12cykloalkyl eller monovalente radikal eventuelt kan være substituert med én, eller hvor mulig to, tre eller flere substituenter valgt fra gruppen bestående av C1-4alkyl, C1-4alkyloksy, halo eller hydroksy; Q representerer Het1 eller Ar2 hvori nevnte C3-8sykloalkyl, Het1 eller Ar2 eventuelt er substituert med én eller hvor mulig to eller flere substituenter valgt fra halo, C1-4alkyl, C1-4alkyloksy, hydroksy, nitro, NR5R6, C1-4alkyloksy substituert med én eller hvor mulig to, tre eller flere substituenter hver uavhengig valgt fra hydroksykarbonyl, Het2 og NR7R8, og C1-4alkyl substituert med én eller hvor mulig to eller tre halosubstituenter, fortrinnsvis trifluormetyl; R5 og R6 representerer hver uavhengig hydrogen, C1-4alkyl, eller C1-4alkyl substituert med fenyl; R7 og R8 representerer hver uavhengig hydrogen eller C1-4alkyl; R9 og R10 representerer hver uavhengig hydrogen, C1-4alkyl eller C1-4alkyloksykarbonyl; L representerer C1-4alkyl; Het1 representerer en heterocykel valgt fra pyridinyl, tiofenyl eller 1,3-benzodioksolyl; Het2 representerer piperidinyl, pyrrolidinyl eller morfolinyl; Ar2 representerer fenyl, naftyl eller indenyl.
NO20053596A 2002-12-23 2005-07-22 Adamantylacetamider som 11-beta hydroksysteroid-dehydrogenaseinhibitorer NO331456B1 (no)

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PCT/EP2002/014832 WO2004056744A1 (en) 2002-12-23 2002-12-23 Adamantyl acetamides as hydroxysteroid dehydrogenase inhibitors
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