AR048320A1 - Derivados de 5-amino-4-hidroxi-7-(1h-indolilmetil)-8-metilnonanamida - Google Patents

Derivados de 5-amino-4-hidroxi-7-(1h-indolilmetil)-8-metilnonanamida

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Publication number
AR048320A1
AR048320A1 ARP050101073A ARP050101073A AR048320A1 AR 048320 A1 AR048320 A1 AR 048320A1 AR P050101073 A ARP050101073 A AR P050101073A AR P050101073 A ARP050101073 A AR P050101073A AR 048320 A1 AR048320 A1 AR 048320A1
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Argentina
Prior art keywords
alkyl
alkoxy
oxo
amino
pyrimidinyl
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ARP050101073A
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English (en)
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Speedel Experimenta Ag
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • 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
    • C07C237/04—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
    • C07C237/06—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 having the nitrogen atoms of the carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/12—Drugs for disorders of the urinary system of the kidneys
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/02—Ophthalmic agents
    • A61P27/06—Antiglaucoma agents or miotics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/04—Inotropic agents, i.e. stimulants of cardiac contraction; Drugs for heart failure
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/12—Antihypertensives
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • 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
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D209/00—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D209/02—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
    • C07D209/04—Indoles; Hydrogenated indoles
    • C07D209/10—Indoles; Hydrogenated indoles with substituted hydrocarbon radicals attached to carbon atoms of the hetero ring
    • C07D209/12—Radicals substituted by oxygen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D231/00—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
    • C07D231/54—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings condensed with carbocyclic rings or ring systems
    • C07D231/56—Benzopyrazoles; Hydrogenated benzopyrazoles
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
    • C07D405/12—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
    • C07D409/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a chain containing hetero atoms as chain links

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Veterinary Medicine (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Ophthalmology & Optometry (AREA)
  • Urology & Nephrology (AREA)
  • Communicable Diseases (AREA)
  • Virology (AREA)
  • Vascular Medicine (AREA)
  • Oncology (AREA)
  • Hospice & Palliative Care (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Indole Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)

Abstract

Proceso para su preparacion y uso de estos compuestos como medicamentos, especialmente como inhibidores de renina. Reivindicacion 1: Compuestos de la formula general en la cual: X es -CH2- o >CH-OH; A) R1 es un radical heterociclilo opcionalmente sustituido o un radical hidrocarbonado no saturado policíclico opcionalmente sustituido cuando X es hidroximetileno; o B) R1 es un radical heterociclilo o un radical hidrocarbonado no saturado policíclico que está sustituido con de uno a cuatro radicales seleccionados de alquilo C1-6, cicloalquilo C3-8, cicloalcoxilo C3-8, cicloalcoxiC3-8-alquiloC1-6, cicloalcoxiC3-6-alcoxiloC1-6, alquilC1-6-amino, dialquilC1-6-amino, amino-alquiloC1-6, amino-alcoxiloC2-7, polihaloalquilo C1-6, polihaloalcoxilo C2-7, nitro, amino, alquenilo C2-6, alcoxilo C1-6, alcanoiloxi C1-6, hidroxilo, halogeno, ciano, carbamoilo, carboxilo y alquilenC1-6-dioxilo, fenilo, fenoxilo, fenilo, fenil-alquiloC1-6 o fenil-alcoxiloC1-6 opcionalmente sustituido con halogeno, alquilo C1-6, alcoxilo C1-6, hidroxilo, alquilC1-6-amino, dialquilC1-6-amino, alcoxiC1-6-carbonilo, hidroxi-alquiloC1-6 o trifluorometilo, piridilcarbonilamino-alquiloC1-6, alqueniloxilo C2-7, alcoxiC1-6-alcoxiloC1-6, alcoxiC1-6-alcoxi- C1-6-alquiloC1-6, metoxibenciloxilo, hidroxibenciloxilo, metilendioxibenciloxilo, dioxolanil-alcoxiloC1-6, cicloalquilC3-6-alquiloC1-6, cicloalquilC3-8-alcoxiloC1-6, hidroxi-alcoxiloC2-7, carbamoiloxi-alcoxiloC2-7, piridilcarbamoiloxi-alcoxiloC2-7, benzoiloxi-alcoxiloC2-7, alcoxiC1-6-carbonilo, alquilC1-6-carbonilamino, alquilC1-6-carbonilamino-alquiloC1-6, alquilC1-6-carbonilamino-alcoxiloC2-7, (N-alquilC1-6)-alquilC1-6-carbonilamino-alquiloC1-6, (N-alquilC1-6)-alquilC1-6-carbonilamino- alcoxiloC2-7, cicloalquilC3-8-carbonilamino-alquiloC1-6, cicloalquilC3-8-carbonilamino-alcoxiloC2-7, alcoxiC1-6-alquiloC1-6, hidroxi-alquiloC1-6, hidroxi-alcoxiC2-7-alquiloC1-6, hidroxi-alcoxiC1-6-alcoxiloC1-6, alcoxiC1-6-carbonilamino-alquiloC1-6, alcoxiC1-6-carbonil-amino-alcoxiloC2-7, alquilC1-6-aminocarbonilamino-alquiloC1-6, alquilC1-6-aminocarbonilamino-alcoxiloC2-7, alquilC1-6-aminocarbonil-alquiloC1-6, alquilC1-6-aminocarbonil-alcoxiloC1-6, alquilC1-6-aminocarbonil-alcoxiC1-6-alquiloC1- 6, dialquilC1-6-aminocarbonil-alquiloC1-6, dialquilC1-6-amino-carbonil-alcoxiloC1-6, alquilC1-6-carboniloxi-alquiloC1-6, alquilC1-6-carboniloxi-alcoxiloC1-6, ciano-alquiloC1-6, ciano-alcoxiloC1-6, 2-oxo-oxazolidinil-alquiloC1-6, 2-oxo-oxazolidinil- alcoxiloC1-6, alcoxiC1-6-carbonil-alquiloC1-6, alcoxiC1-6-carbonil alcoxiloC1-6, alquilC1-6-sulfonilamino-alquiloC1-6, alquilC1-6-sulfonilamino-alcoxiloC1-6, (N-alquilC1-6)-alquilC1-6-sulfonilamino-alquiloC1-6, (N-alquilC1-6)-alquilC1-6- sulfonilamino-alcoxiloC2-7, alquilC1-6-amino-alquiloC1-6, alquilC1-6-amino-alcoxiloC2-7, dialquilC1-6-amino-alquilC1-6, dialquilC1-6-amino-alcoxiloC2-7, alquilC1-6-sulfonil-alquiloC1-6, alquilC1-6-sulfonil-alcoxiloC1-6, carboxi-alquioC1-6, carboxi- alcoxiloC1-6, carboxi-alcoxiC1-6-alquiloC1-6, alcoxiC1-6-alquilC1-6-carbonilo, acil-alcoxiC1-6-alquiloC1-6, (N-alquilC1-6)-alcoxiC1-6-carbonilamino, (N-hidroxi)-alquilC1-6-amino-carbonil-alquiloC1-6, (N-hidroxi)-alquilC1-6-aminocarbonil-alcoxiloC1- 6, (N-hidroxi)-aminocarbonil-alquiloC1-6, (N-hidroxi)-aminocarbonil-alcoxiloC1-6, alcoxiC1-6-aminocarbonil-alquiloC1-6, 6-alcoxi-aminocarbonil-alcoxiloC1-6, (N-alcoxiC1-6)-alquilC1-6-aminocarbonil-alquiloC1-6, (N-alcoxiC1-6)-alquilC1-6-aminocarbonil- alcoxiloC1-6, (N-acil)-alcoxiC1-6-alquilC1-6-amino, alcoxiC1-6-alquilC1-6-carbamoilo, (N-alquilC1-6)-alcoxiC1-6-alquilC1-6-carbamoilo, alcoxiC1-6-alquilC1-6-carbonilo, alcoxiC1-6-alquilC1-6-carbonil-amino, (N-alquilC1-6)-alcoxiC1-6-alquilC1-6- carbonilamino, 1-alcoxiC1-6-alquilC1-6-imidazol-2-ilo, 1-alcoxiC1-6-alquilC1-6-tetrazol-5-ilo, 5-alcoxiC1-6-alquilC1-6-tetrazol-1-ilo, 2-alcoxiC1-6-alquilC1-6-4-oxoimidazol-1-ilo, carbamoil-alquiloC1-6, carbamoil-alcoxiloC1-6, alquilC1-6-carbamoilo, dialquilC1-6-carbamoilo, alquilC1-6-sulfonilo, alquilC1-6-amidinilo, acetamidinil-alquiloC1-6, O-metil-oximil-alquil1C1-6, O,N-dimetilhidroxilamino-alquiloC1-6, cicloalquilC3-6-alcanoiloC1-6, aril-alcanoiloC1-6 o heterociclil-alcanoiloC1-6, y también piridilo, piridiloxilo, piridiltio, piridilamino, piridil-alquiloC1-6, piridil-alcoxiloC1-6, pirimidilo, pirimidiniloxilo, pirimidiniltio, pirimidinilamilo, pirimidinil-alquiloC1-6, pirimidinil-alcoxiloC1-6, tienilo, tienil-alquiloC1-6, tienil-alcoxiloC1-6, furilo, furil-alquiloC1-6 o furil-alcoxiloC1-6 sustituidos opcionalmente con halogeno, alquilo C1-6, alcoxilo C1-6 o dihidroxi-alquilC1-6-aminocarbonilo, piperidinoalquilo, piperidinoalcoxilo, piperidinoalcoxialquilo, morfolinoalquilo, morfolinoalcoxilo, morfolinoalcoxialquilo, piperazinoalquilo, piperazino-alcoxilo, piperazinoalcoxi-alquilo, [1,2,4]triazol-1-il-alquilo, [1,2,4]triazol-1-il-alcoxilo, [1,2,4]triazol-4-il-alquilo, [1,2,4]triazol-4-il-alcoxilo, [1,2,4]oxadiazol-5-il-alquilo, [1,2,4]oxadiazol-5-il-alcoxilo, 3-metil[1,2,4]oxadiazol-5-il-alquilo, 3-metil[1,2,4]oxadiazol-5-il-alcoxilo, 5-metil[1,2,4]-oxadiazol-3-il-alquilo, 5-metil[1,2,4]oxadiazol-3-il-alcoxilo, tetrazol-1-il-alquilo, tetrazol- 1-il-alcoxilo, tetrazol-2-il-alquilo, tetrazol-2-il-alcoxilo, tetrazol-5-il-alquilo, tetrazol-5-il-alcoxilo, 5-metil-tetrazol-1-il-alcoxilo, 5-metil-tetrazol-1-il-alcoxilo, tiazol-4-il-alquilo, tiazol-4-il-alcoxilo, oxazol-4-il-alquilo, oxazol-4-il- alcoxilo, 2-oxo-pirrolidinilo-alquilo, 2-oxopirrolidinilo-alcoxilo, imidazol-alquilo, imidazol-alcoxilo, 2-metilimidazol-2-il-alquilo, 2-metilimidazolil-alcoxilo o N-metilpiperazino-alquilo, N-metilpiperazino-alcoxilo, N-metilpiperazino-alcoxi- alquilo, dioxolanilo, dioxanilo, ditiolanilo, ditianilo, pirrolidinilo, piperidinilo, piperazinilo, pirrolilo, 4-metil-piperazinilo, morfolinilo, tiomorfolinilo, 2-hidroximetilpirrolidinilo, 3-hidroxi-pirrolidin-ilo, 3,4-dihidroxipirrolidinilo, 3- acetamidometilpirrolidinilo, 3-alcoxiC1-6-alquilC1-6-pirrolidinilo, 4-hidroxi-piperidinilo, 4-oxopiperidinilo, 3,5-dimetilmorfolinilo, 4,4-dioxo-tiomorfolinilo, 4-oxo-tiomorfonilo, 2,6-dimetilmorfolinilo, 2-oxoimidazolidinilo, 2-oxooxazolidinilo, 2- oxo-pirrolidinilo, 2-oxo[1,3]oxazinilo, 2-oxotetrahidropirimidinilo, y el radical -O-CH2CH(OH)CH2NRx en donde NRx, es un radical mono- o di-alquilC1-6-amino, piperidino, morfolino, piperazino o N-metilpiperazino; donde, en el caso de que R1 sea naftilo o ciclohexenofenilo, al menos el sistema anular no unido a X está sustituido como se específica; o C) R1 es pirazinilo, triazolilo, imidazolilo, benzotiazolilo, piranilo, tetrahidropiranilo, azetidinilo, morfolinilo, quinazolinilo, quinoxalinilo, isoquinolilo, benzo[b]tienilo, isobenzofuranilo, bencimidazolilo, 2-oxobencimidazolilo, oxazolilo, tiazolilo, pirrolilo, pirazolilo, triazinilo, dihidrobenzofuranilo, 2-oxodihidrobenzo[d][1,3]oxazinilo, 4-oxodihidroimidazolilo, 5-oxo- 4H-[1,2,4]triazinilo, 3-oxo-4H-benzo[1,4]tiazinilo, tetrahidroquinoxalinilo, 1,1,3-trioxohidro-2H-1lambda6-benzo[1,4]tiazinilo, 1-oxopiridilo, dihidro-3H-benzo[1,4]oxazinilo, 2-oxotetrahidrobenzo[e][1,4]diazepinilo, 2-oxodihidro- benzo[e][1,4]diazepinilo, 1H-pirrolizinilo, ftalazinilo, 1-oxo-3H-isobenzofuranilo, 4-oxo-3H-tieno[2,3-d]pirimidinilo, 3-oxo-4H-benzo[1,4]oxazinilo, [1,5]naftiridilo, dihidro-2H-benzo[1,4]tiazinilo, 1,1-dioxodihidro-2H-benzo-[1,4]tiazinilo, 2-oxo-1H- pirido[2,3-d][1,4]oxazinilo, dihidro-1H-pirido[2,3-b]-[1,4]oxazinilo, 1H-pirrol[2,3-b]piridilo, benzo[1,3]dioxolilo, benzooxazolilo, 2-oxo-benzooxazolilo, 2-oxo-1,3-dihidro-indol-ilo, 2,3-dihidroindolilo, indazolilo, benzofuranilo, dioxolanilo, dioxanilo, ditiolanilo, ditianilo, pirrolidinilo, piperidinilo, piperazinilo, 4-metil-piperazinilo, morfolinilo, tiomorfolinilo, 2-hidroximetilpirrolidinilo, 3-hidroxipirrolidinilo, 3,4-dihidroxi-pirrolidinilo, 4-hidroxipiperidinilo, 4- oxopiperidinilo, 3,5-dimetilmorfolinilo, 4,4-dioxo-tiomorfolin-ilo, 4-oxotiomorfolinilo, 2,6-dimetilmorfolinilo, tetrahidropiranilo, 2-oxo-imidazolidin-ilo, 2-oxo-oxazolidinilo, 2-oxo-piperidinilo, 2-oxo-pirrolidinilo, 2-oxo[1,3]-oxazinilo, 2- oxoazepanilo o 2-oxotetrahidropirimidinilo; R2 es alquilo C1-6 o cicloalquilo C3-8; R3 es independientemente entre sí H, alquilo C1-6 o alcanoilo C1-6; R4 es alquilo C1-6, cicloalquilo C3-8, alquenilo C2-6 o aril-alquiloC1-6 sin sustituir o sustituido; R5 es alquilo C1-6, hidroxialquilo C1-6, alcoxiC1-6-alquiloC1-6, alcanoiloxiC1-6-alquiloC1-6, aminoalquilo C1-6, alquilC1-6-amino-alquiloC1-6, dialquilC1-6-amino-alquiloC1-6, alcanoilC1-6-amido-alquiloC1-6, HO(O)C-alquiloC1-6, alquilC1-6- O-(O)C-alquiloC1-6, H2N-C(O)-alquiloC1-6, alquilC1-6-NH-C(O)-alquiloC1-6, (alquilC1-6)2-N-C(O)-alquiloC1-6, cicloalquilo C3-6 sin sustituir o sustituido o heterociclilo sin sustituir o sustituido; y su sal, en particular su sal farmacéuticamente util.
ARP050101073A 2004-03-19 2005-03-18 Derivados de 5-amino-4-hidroxi-7-(1h-indolilmetil)-8-metilnonanamida AR048320A1 (es)

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US (1) US7851634B2 (es)
EP (4) EP1724259A1 (es)
JP (1) JP2007529474A (es)
CN (1) CN1934083A (es)
AR (1) AR048320A1 (es)
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EP1764098A1 (en) * 2005-09-17 2007-03-21 Speedel Experimenta AG Diaminoalcohols derivatives for the treatment of Alzheimer, malaria, HIV
BRPI0617166A2 (pt) 2005-09-17 2011-07-12 Speedel Experimenta Ag derivados de 5-amino-4-hidróxi-7-(imidazo[1,2-a]piridin-6-ilmetil)-8-me til-nonamidia e compostos relacionados como inibidores de renina para o tratamento de hipertensão
GB0521083D0 (en) * 2005-10-17 2005-11-23 Novartis Ag Organic compounds
BRPI0620736A2 (pt) 2005-12-30 2011-12-20 Novartis Ag compostos orgánicos
JP2009525304A (ja) * 2006-01-30 2009-07-09 シュペーデル・エクスペリメンタ・アーゲー α，β−不飽和化合物からのアルコールの立体選択的製造方法
TW200831463A (en) * 2006-09-12 2008-08-01 Speedel Experimenta Ag Nitrate esters of aminoalcohols
EP1911762A1 (en) * 2006-10-04 2008-04-16 Speedel Experimenta AG Amino alcohols and their use as renin inhibitors
EP1921069A1 (de) * 2006-11-08 2008-05-14 Speedel Experimenta AG Verfahren zur Herstellung von 2-Alkyl-3-heterocyclyl-prop-2-en-1-olen
EP1939182A1 (de) * 2006-12-22 2008-07-02 Speedel Experimenta AG Verfahren zur Herstellung von (R oder S)-2-Alkyl-3-heterocyclyl-1-propanolen
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EP1712548A3 (en) 2006-11-02
US7851634B2 (en) 2010-12-14
EP1712548A2 (en) 2006-10-18
BRPI0508961A (pt) 2007-08-14
TW200536539A (en) 2005-11-16
EP1717226B1 (en) 2009-01-21
PL1717226T3 (pl) 2009-07-31
EP1724259A1 (en) 2006-11-22
ES2320030T3 (es) 2009-05-18
IL178100A0 (en) 2006-12-31
PT1717226E (pt) 2009-04-03
EP1699762A1 (en) 2006-09-13
US20080280895A1 (en) 2008-11-13
CN1934083A (zh) 2007-03-21
EP1717226A1 (en) 2006-11-02
CA2560199A1 (en) 2005-09-29
JP2007529474A (ja) 2007-10-25
DE602005012481D1 (de) 2009-03-12
WO2005090305A1 (en) 2005-09-29

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