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PE20061325A1 - Derivados de pirrolidina como inhibidores de la renina - Google Patents

Derivados de pirrolidina como inhibidores de la renina

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Publication number
PE20061325A1
PE20061325A1 PE2006000322A PE2006000322A PE20061325A1 PE 20061325 A1 PE20061325 A1 PE 20061325A1 PE 2006000322 A PE2006000322 A PE 2006000322A PE 2006000322 A PE2006000322 A PE 2006000322A PE 20061325 A1 PE20061325 A1 PE 20061325A1
Authority
PE
Peru
Prior art keywords
substituted
unsustituted
rent
chre
pyrrolidin
Prior art date
Application number
PE2006000322A
Other languages
English (en)
Inventor
Claus Ehrhardt
Osamu Irie
Juergen Klaus Maibaum
Holger Sellner
Nils Ostermann
Edwige Liliane Jeanne Lorthiois
Original Assignee
Novartis Ag
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 Novartis Ag filed Critical Novartis Ag
Publication of PE20061325A1 publication Critical patent/PE20061325A1/es

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • 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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    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
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    • A61K31/33—Heterocyclic compounds
    • A61K31/335—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
    • A61K31/34—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having five-membered rings with one oxygen as the only ring hetero atom, e.g. isosorbide
    • A61K31/341—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having five-membered rings with one oxygen as the only ring hetero atom, e.g. isosorbide not condensed with another ring, e.g. ranitidine, furosemide, bufetolol, muscarine
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    • A61K31/33—Heterocyclic compounds
    • A61K31/335—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
    • A61K31/35—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having six-membered rings with one oxygen as the only ring hetero atom
    • A61K31/351—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having six-membered rings with one oxygen as the only ring hetero atom not condensed with another ring
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    • A61K31/352—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having six-membered rings with one oxygen as the only ring hetero atom condensed with carbocyclic rings, e.g. methantheline 
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    • A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
    • A61K31/4025—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil not condensed and containing further heterocyclic rings, e.g. cromakalim
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    • A61K31/404—Indoles, e.g. pindolol
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    • A61K31/416—1,2-Diazoles condensed with carbocyclic ring systems, e.g. indazole
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    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4409—Non condensed pyridines; Hydrogenated derivatives thereof only substituted in position 4, e.g. isoniazid, iproniazid
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    • A61K31/445—Non condensed piperidines, e.g. piperocaine
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    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
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  • Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)

Abstract

REFERIDA A UN COMPUESTO DE PIRROLIDINA DE FORMULA (I); DONDE R1 ES ALQUILO INSUSTITUIDO O SUSTITUIDO, ARILO MONOCICLICO O BI-CICLICO INSUSTITUIDO O SUSTITUIDO, ENTRE OTROS; R2 ES UN ALQUILO INSUSTITUIDO O SUSTITUIDO, ARILO MONO O BI-CICLICO INSUSTITUIDO O SUSTITUIDO, CICLOALQUILO MONO O BI-CICLICO INSUSTITUIDO O SUSTITUIDO, ENTRE OTROS; R3 ES -CHRe-O-Ra, -CHRe-NRbRc, -CHRe-S(O)m-Rd, ENTRE OTROS; Ra ES ALQUILO INSUSTITUIDO O SUSTITUIDO, ARILO MONO O BI-CICLICO INSUSTITUIDO O SUSTITUIDO, ENTR EOTROS; Rb Y Rc SON COMO Ra, CON LA CONDICION DE QUE DE PREFERENCIA NO MAS DE UNO DE Rb Y Rc SEA ACILO, O Rb Y Rc PUEDEN FORMAR JUNTOS UN ANILLO DE 3 A 7 MIEMBROS QUE CONTENGA N, EL CUAL PUEDE ESTAR SUSTITUIDO O INSUSTITUIDO; Re ES H, ARILO MONO O BI-CICLICO, ENTRE OTROS; m ES 0, 1 O 2; R4 Y R5 SON H, ALQUILO INSUSTITUIDO O SUSTITUIDO, OH, ENTRE OTROS; T ES METILENO, METILENO MONO-SUSTITUIDO POR ALQUILO, CARBONILO O TIOCARBONILO. SON COMPUESTOS PREFERIDOS: N-((3S*,4S*)-4-{[(3-ACETIL-AMINO-3-METIL-BUTIRIL)-CICLOPROPIL-AMINO]-METIL}-PIRROLIDIN-3-ILMETIL)-N-ISOPROPIL-4-METOXI-3-(3-METOXI-PROPOXI)-BENZAMIDA, N-((3S*,4S*)-4-({CICLOPROPIL-[2-(2-OXO-PIRROLIDIN-1-IL)-ACETIL]-AMINO}-METIL)-PIRROLIDIN-3-ILMETIL]-N-ISOPROPIL-4-METOXI-3-(3-METOXI-PROPOXI)-BENZAMIDA, ENTRE OTROS. TAMBIEN ESTA REFERIDA A UNA COMPOSICION Y A UN PROCESO DE PREPARACION. DICHOS COMPUESTOS SON INHIBIDORES DE LA RENINA Y SON UTILES EN EL TRATAMIENTO DE DE HIPERTENSION, ARTEROESCLEROSIS, SINDROME CORONARIO, ENTRE OTROS
PE2006000322A 2005-03-23 2006-03-23 Derivados de pirrolidina como inhibidores de la renina PE20061325A1 (es)

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