AR059031A1 - Combinacion de derivados de triazina e inhibidores de la hmg- coa reductasa - Google Patents

Combinacion de derivados de triazina e inhibidores de la hmg- coa reductasa

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Publication number
AR059031A1
AR059031A1 ARP070100137A ARP070100137A AR059031A1 AR 059031 A1 AR059031 A1 AR 059031A1 AR P070100137 A ARP070100137 A AR P070100137A AR P070100137 A ARP070100137 A AR P070100137A AR 059031 A1 AR059031 A1 AR 059031A1
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AR
Argentina
Prior art keywords
alkoxy
alkyl
aryl
halogen
optionally substituted
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ARP070100137A
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English (en)
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Gerard Moinet
Daniel Cravo
Didier Mesangeau
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Merck Patent Gmbh
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Publication of AR059031A1 publication Critical patent/AR059031A1/es

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    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/40Heterocyclic 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/21Esters, e.g. nitroglycerine, selenocyanates
    • A61K31/215Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids
    • A61K31/22Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids of acyclic acids, e.g. pravastatin
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/335Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
    • A61K31/35Heterocyclic 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
    • A61K31/351Heterocyclic 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/40Heterocyclic 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
    • A61K31/403Heterocyclic 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 condensed with carbocyclic rings, e.g. carbazole
    • A61K31/404Indoles, e.g. pindolol
    • A61K31/405Indole-alkanecarboxylic acids; Derivatives thereof, e.g. tryptophan, indomethacin
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic 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
    • A61K31/47Quinolines; Isoquinolines
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/53Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with three nitrogens as the only ring hetero atoms, e.g. chlorazanil, melamine
    • AHUMAN NECESSITIES
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    • A61P13/00Drugs for disorders of the urinary system
    • A61P13/12Drugs for disorders of the urinary system of the kidneys
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • AHUMAN NECESSITIES
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    • A61P27/00Drugs for disorders of the senses
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    • AHUMAN NECESSITIES
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    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • A61P3/06Antihyperlipidemics
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    • A61P3/08Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
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    • AHUMAN NECESSITIES
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    • AHUMAN NECESSITIES
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    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/12Antihypertensives

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  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
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Abstract

Reivindicacion 1: Composicion farmacéutica que comprende, como principio activo: i) un inhibidor de la HMG-CoA reductasa, ii) un derivado de la triazina de la formula (1) en donde: R1, R2, R3 y R4 se seleccionan en forma independiente entre los grupos siguientes: H; -alquilo C1-20 opcionalmente substituido con halogeno, alquilo C1-5, alcoxi C1-5, cicloalquilo C3-8; -alquenilo C2-20 opcionalmente substituido con halogeno, alquilo C1-5 o alcoxi C1-5; -alquinilo C2-20 opcionalmente substituido con halogeno, alquilo C1-5 o alcoxi C1-5; -cicloalquilo C3-8 opcionalmente substituido con alquilo C1-5 o alcoxi C1-5; -heterocicloalquilo C3-8 con uno o más heteroátomos seleccionados entre N, O y S y opcionalmente substituido con alquilo C1-5 o alcoxi C1-5; -aril C6-14alquilo C1-20 opcionalmente substituido con amino, hidroxilo, tio, halogeno, alquilo C1-5, alcoxi C1-5, alquiltio C1-5, alquilamino C1-5, ariloxi C6-14, aril C6-14alcoxi C1-5, ciano, trifluorometilo, carboxilo, carboximetilo o carboxietilo; -arilo C6-14 opcionalmente substituido con amino, hidroxilo, tio, halogeno, alquilo C1-5, alcoxi C1-5, alquiltio C1-5, alquilamino C1-5, ariloxi C6-14, aril C6-14alcoxi C1-5, ciano, trifluorometilo, carboxilo, carboximetilo o carboxietilo; -heteroarilo C1-13 con uno o más heteroátomos seleccionados entre N, O y S y opcionalmente substituido con amino, hidroxilo, tio, halogeno, alquilo C1-5, alcoxi C1-5, alquiltio C1-5, alquilamino C1-5, ariloxi C6-14, aril C6-14alcoxi C1-5, ciano, trifluorometilo, carboxilo, carboximetilo o carboxietilo; R1 y R2, por un lado, y R3 y R4, por otro lado, pueden formar con el átomo de nitrogeno un anillo de n-miembros (n es entre 3 y 8) que contiene opcionalmente uno o más heteroátomos seleccionados entre N, O y S y puede estar substituido por uno o más de los grupos siguientes: amino, hidroxilo, tio, halogeno, alquilo C1-5, alcoxi C1-5, alquiltio C1-5, alquilamino C1-5, ariloxi C6-14, aril C6-14-alcoxi C1-5, ciano, trifluorometilo, carboxilo, carboximetilo o carboxietilo; R5 y R6 se seleccionan en forma independiente entre los grupos siguientes: -H; -alquilo C1-20 opcionalmente substituido con amino, hidroxilo, tio, halogeno, alquilo C1-5, alcoxi C1-5, alquiltio C1-5, alquilamino C1-5, ariloxi C6-14, aril C6-14alcoxi C1-5, ciano, trifluorometilo, carboxilo, carboximetilo o carboxietilo; -alquenilo C2-20 opcionalmente substituido con amino, hidroxilo, tio, halogeno, alquilo C1-5, alcoxi C1-5, alquiltio C1-5, alquilamino C1-5, ariloxi C6-14, aril C6-14alcoxi C1-5, ciano, trifluorometilo, carboxilo, carboximetilo o carboxietilo; -alquinilo C2-20 opcionalmente substituido con amino, hidroxilo, tio, halogeno, alquilo C1-5, alcoxi C1-5, alquiltio C1-5, alquilamino C1-5, ariloxi C6-14, aril C6-14alcoxi C1-5, ciano, trifluorometilo, carboxilo, carboximetilo o carboxietilo; -cicloalquilo C3-8 opcionalmente substituido con amino, hidroxilo, tio, halogeno, alquilo C1-5, alcoxi C1-5, alquiltio C1-5, alquilamino C1-5, ariloxi C6-14, aril C6-14alcoxi C1-5, ciano, trifluorometilo, carboxilo, carboximetilo o carboxietilo; -heterocicloalquilo C3-8 con uno o más heteroátomos seleccionados entre N, O y S y opcionalmente substituido con amino, hidroxilo, tio, halogeno, alquilo C1-5, alcoxi C1-5, alquiltio C1-5, alquilamino C1-5, ariloxi C6-14, aril C6-14alcoxi C1-5, ciano, trifluorometilo, carboxilo, carboximetilo o carboxietilo; -arilo C6-14 opcionalmente substituido con amino, hidroxilo, tio, halogeno, alquilo C1-5, alcoxi C1-5, alquiltio C1-5, alquilamino C1-5, ariloxi C6-14, aril C6-14alcoxi C1-5, ciano, trifluorometilo, carboxilo, carboximetilo o carboxietilo; heteroarilo C1-13 con uno o más heteroátomos seleccionados entre N, O y S y opcionalmente substituido con amino, hidroxilo, tio, halogeno, alquilo C1-5, alcoxi C1-5, alquiltio C1-5, alquilamino C1-5, ariloxi C6-14, aril C6-14alcoxi C1-5, ciano, trifluorometilo, carboxilo, carboximetilo o carboxietilo; aril C6-14alquilo C1-5 opcionalmente substituido con amino, hidroxilo, tio, halogeno, alquilo C1-5, alcoxi C1-5, alquiltio C1-5, alquilamino C1-5, ariloxi C6-14, aril C6-14alcoxi C1-5, ciano, trifluorometilo, carboxilo, carboximetilo o carboxietilo, R5 y R6 pueden formar con el átomo de carbono al cual están unidos un anillo de m miembros (m es entre 3 y 8) que contiene opcionalmente uno o más heteroátomos seleccionados entre N, O y S y pueden estar substituidos con amino, hidroxilo, tio, halogeno, alquilo C1-5, alcoxi C1-5, alquiltio C1-5, alquilamino C1-5, ariloxi C6-14, aril C6-14alcoxi C1-5, ciano, trifluorometilo, carboxilo, carboximetilo o carboxietilo, o pueden formar con el átomo de carbono un residuo policíclico C10-30 opcionalmente substituido con amino, hidroxilo, tio, halogeno, alquilo C1-5, alcoxi C1-5, alquiltio C1-5, alquilamino C1-5, ariloxi C6-14, aril C6-14alcoxi C1-5, ciano, trifluorometilo, carboxilo, carboximetilo o carboxietilo, R5 y R6 juntos pueden también representar grupo =O o =S, el átomo de nitrogeno de un grupo heterocicloalquilo o heteroarilo puede estar substituido con un grupo alquilo C1-5, cicloalquilo C3-8, arilo C6-14, aril C6-14alquilo C1-5 o acilo C1-6, y también las formas racémicas, tautomeras, enantiomeras, diastereoisomeros, epímeros y polimorfos, y mezclas de los mismos, y sus sales aceptables para uso farmacéutico, y uno o más excipientes aceptables para uso farmacéutico.
ARP070100137A 2006-01-13 2007-01-12 Combinacion de derivados de triazina e inhibidores de la hmg- coa reductasa AR059031A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
FR0600343A FR2896158B1 (fr) 2006-01-13 2006-01-13 Combinaison de derives de triazine et d'inhibiteurs de la hmg-coa reductase.

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AR059031A1 true AR059031A1 (es) 2008-03-12

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US (1) US20100158999A1 (es)
EP (1) EP1978951A2 (es)
JP (1) JP2009523141A (es)
KR (1) KR20080085208A (es)
CN (1) CN101355935A (es)
AR (1) AR059031A1 (es)
AU (1) AU2006334733A1 (es)
BR (1) BRPI0621420A2 (es)
CA (1) CA2636840A1 (es)
EA (1) EA200801666A1 (es)
FR (1) FR2896158B1 (es)
IL (1) IL192594A0 (es)
WO (1) WO2007079916A2 (es)
ZA (1) ZA200806937B (es)

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US6949245B1 (en) * 1999-06-25 2005-09-27 Genentech, Inc. Humanized anti-ErbB2 antibodies and treatment with anti-ErbB2 antibodies
KR101085157B1 (ko) * 2007-08-31 2011-11-18 한국화학연구원 1,3,5-트리아진-2,4,6-트리아민 화합물 또는 그의 약학적으로 허용 가능한 염, 및 이를 포함하는 약학적 조성물
BRPI0922650A2 (pt) * 2008-12-12 2017-07-11 Poxel Composto, composição farmacêutica, uso de pelo menos um composto, métodos para tratar doenças, para diagnosticar nefropatia diabética, e para triar compostos, e, uso de sinaptopodina
FR2948028B1 (fr) * 2009-07-17 2011-12-02 Merck Sante Sas Association d'un inhibiteur de l'echangeur sodium-proton et d'un derive amine de dihydro-1,3,5-triazine
EP2602249B1 (en) * 2011-12-06 2015-08-12 F.I.S. Fabbrica Italiana Sintetici S.p.A. Synthesis of rosuvastatin by means of co-crystals
WO2019236844A1 (en) 2018-06-06 2019-12-12 Metavant Sciences Gmbh Methods of treating subjects having diabetes with chronic kidney disease
CN112218623A (zh) * 2018-06-14 2021-01-12 博希尔公司 用于治疗糖尿病的包含三嗪衍生物的薄膜包衣片剂
KR20220113942A (ko) * 2019-12-13 2022-08-17 스미토모 파마 가부시키가이샤 제조성 및 용출성이 우수한 소형 정제

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JP3651816B2 (ja) * 1995-07-03 2005-05-25 三共株式会社 動脈硬化症予防および治療剤
FR2804113B1 (fr) * 2000-01-26 2004-06-18 Lipha Derives animes de dihydro-1,3,5-triazine et leurs applications en therapeutique
FR2853650B1 (fr) * 2003-04-10 2006-07-07 Merck Sante Sas Procede de dedoublement d'amines utiles pour le traitement de desordres associes au syndrome d'insulino-resistance
EP1510208A1 (en) * 2003-08-22 2005-03-02 Fournier Laboratories Ireland Limited Pharmaceutical composition comprising a combination of metformin and statin

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EP1978951A2 (en) 2008-10-15
FR2896158B1 (fr) 2008-09-12
ZA200806937B (en) 2009-07-29
WO2007079916A2 (en) 2007-07-19
FR2896158A1 (fr) 2007-07-20
BRPI0621420A2 (pt) 2011-12-06
CN101355935A (zh) 2009-01-28
AU2006334733A1 (en) 2007-07-19
EA200801666A1 (ru) 2008-12-30
US20100158999A1 (en) 2010-06-24
IL192594A0 (en) 2009-09-22
KR20080085208A (ko) 2008-09-23
CA2636840A1 (en) 2007-07-19
JP2009523141A (ja) 2009-06-18
WO2007079916A3 (en) 2007-12-06

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