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BR0311338A - Derivados de n-acilaminobenzeno como inibidores seletivos da monoamina oxidade b - Google Patents

Derivados de n-acilaminobenzeno como inibidores seletivos da monoamina oxidade b

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Publication number
BR0311338A
BR0311338A BR0311338-8A BR0311338A BR0311338A BR 0311338 A BR0311338 A BR 0311338A BR 0311338 A BR0311338 A BR 0311338A BR 0311338 A BR0311338 A BR 0311338A
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Prior art keywords
alkyl
hydrogen
alkoxy
halogen
derivatives
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BR0311338-8A
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English (en)
Inventor
Synese Jolidon
Rosa Maria Rodriguez Sarmiento
Andrew William Thomas
Rene Wyler
Original Assignee
Hoffmann La Roche
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Publication date
Application filed by Hoffmann La Roche filed Critical Hoffmann La Roche
Publication of BR0311338A publication Critical patent/BR0311338A/pt

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    • C07C259/00—Compounds containing carboxyl groups, an oxygen atom of a carboxyl group being replaced by a nitrogen atom, this nitrogen atom being further bound to an oxygen atom and not being part of nitro or nitroso groups
    • C07C259/04—Compounds containing carboxyl groups, an oxygen atom of a carboxyl group being replaced by a nitrogen atom, this nitrogen atom being further bound to an oxygen atom and not being part of nitro or nitroso groups without replacement of the other oxygen atom of the carboxyl group, e.g. hydroxamic acids
    • C07C259/06—Compounds containing carboxyl groups, an oxygen atom of a carboxyl group being replaced by a nitrogen atom, this nitrogen atom being further bound to an oxygen atom and not being part of nitro or nitroso groups without replacement of the other oxygen atom of the carboxyl group, e.g. hydroxamic acids having carbon atoms of hydroxamic groups bound to hydrogen atoms or to acyclic carbon atoms
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    • C07C233/15—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 halogen atoms or by nitro or nitroso groups with the substituted hydrocarbon radical bound to the nitrogen atom of the carboxamide group by a carbon atom of a six-membered aromatic ring
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    • C07C233/24—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 six-membered aromatic ring
    • C07C233/25—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 six-membered aromatic ring having the carbon atom of the carboxamide group bound to a hydrogen atom or to a carbon atom of an acyclic saturated carbon skeleton
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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
    • C07C233/33—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 six-membered aromatic ring
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    • C07C233/60—Carboxylic acid amides having carbon atoms of carboxamide groups bound to carbon atoms of rings other than six-membered aromatic rings 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
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    • C07C235/04—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 being acyclic and saturated
    • C07C235/16—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 being acyclic and saturated having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a six-membered aromatic ring
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    • C07C237/02—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
    • C07C237/04—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 being acyclic and saturated
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    • C07C237/00—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups
    • C07C237/02—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
    • 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
    • C—CHEMISTRY; METALLURGY
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    • C07C243/00—Compounds containing chains of nitrogen atoms singly-bound to each other, e.g. hydrazines, triazanes
    • C07C243/10—Hydrazines
    • C07C243/12—Hydrazines having nitrogen atoms of hydrazine groups bound to acyclic carbon atoms
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    • C07C243/24—Hydrazines having nitrogen atoms of hydrazine groups acylated by carboxylic acids
    • C07C243/26—Hydrazines having nitrogen atoms of hydrazine groups acylated by carboxylic acids with acylating carboxyl groups bound to hydrogen atoms or to acyclic carbon atoms
    • C07C243/28—Hydrazines having nitrogen atoms of hydrazine groups acylated by carboxylic acids with acylating carboxyl groups bound to hydrogen atoms or to acyclic carbon atoms to hydrogen atoms or to carbon atoms of a saturated carbon skeleton
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Abstract

"DERIVADOS DE N-ACILAMINOBENZENO COMO INIBIDORES SELETIVOS DA MONOAMINA OXIDASE B". A presente invenção refere-se a derivados N-acilamino arílicos da fórmula geral onde R^ 1^ é halogênio, halogênio-(C~ 1~-C~ 6~)-alquila, ciano, C~ l~-C~ 6~-alcóxi ou halogênio-(C~ l~-C~ 6~)-alcóxi; R^ 21^, R^ 22^, R^ 23^ e R^ 24^ independentemente um do outro são selecionados do grupo que consiste em hidrogênio, C~ l~-C~ 6~ alquila, halogênio, halogênio-(C~ l~-C~ 6~)-alquila, hidróxi, C~ l~-C~ 6~-alcóxi ou -CHO; R^ 3^ é hidrogênio ou C~ 1~-C~ 3~-alquila; R^ 4^, R^ 5^ independentemente um do outro são selecionados do grupo que consiste em hidrogênio, C~ 1~-C~ 6~-alquila, C~ 1~-C~ 6~-alcóxi ou -COO(C~ l~-C~ 6~)-alquila; ou R^ 4^ e R^ 5^ junto com o átomo de C ao qual estão ligados formam um anel C~ 3~-C~ 7~-Cicloalquila; R^ 6^ é -CO-NR^ 7^ R^ 8^; -COO(C~ l~-C~ 6~)alquila, -CN, -NR~ 2~ OU -NHC(O)R; R^ 7^ e R^ 8^ independentemente um do outro são selecionados do grupo que consiste em hidrogênio, C~ l~-C~ 6~-alquila, NH~ 2~ ou hidróxi; R é hidrogênio ou C~ l~-C~ 6~ alquila; n é 0, 1, 2 ou 3, X é -CHRO, -OCHR-, -CH~ 2~S-, -SCH~ 2~,-CH~ 2~CH~ 2~-CH=CH- ou -C=-C-; e sais de adição de ácido farmaceuticamente ativos dos mesmos. Descobriu-se que os compostos de fórmula geral I são inibidores seletivos de monoamina oxidase B e são portanto úteis no tratamento de doenças mediadas por inibidores de monoamina oxidase B, por exemplo para o tratamento do mal de Alzheimer ou demência senil.
BR0311338-8A 2002-05-29 2003-05-20 Derivados de n-acilaminobenzeno como inibidores seletivos da monoamina oxidade b BR0311338A (pt)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
EP02011639 2002-05-29
PCT/EP2003/005297 WO2003099763A1 (en) 2002-05-29 2003-05-20 N-acylaminobenzene dervatives as selective monoamine oxidase b inhibitors

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BR0311338A true BR0311338A (pt) 2005-03-22

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US (3) US6762320B2 (pt)
EP (1) EP1511718B1 (pt)
JP (1) JP4223003B2 (pt)
KR (1) KR100706739B1 (pt)
CN (1) CN100482638C (pt)
AR (1) AR040133A1 (pt)
AT (1) ATE430726T1 (pt)
AU (1) AU2003240681B2 (pt)
BR (1) BR0311338A (pt)
CA (1) CA2486380C (pt)
CY (1) CY1109220T1 (pt)
DE (1) DE60327522D1 (pt)
DK (1) DK1511718T3 (pt)
EA (1) EA009372B1 (pt)
ES (1) ES2324214T3 (pt)
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NO (1) NO329387B1 (pt)
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EP1511718A1 (en) 2005-03-09
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