AR080444A1 - Metodos para la utilizacion de cotransportadores de sodio-glucosa 1 y 2 - Google Patents

Metodos para la utilizacion de cotransportadores de sodio-glucosa 1 y 2

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Publication number
AR080444A1
AR080444A1 ARP110100644A ARP110100644A AR080444A1 AR 080444 A1 AR080444 A1 AR 080444A1 AR P110100644 A ARP110100644 A AR P110100644A AR P110100644 A ARP110100644 A AR P110100644A AR 080444 A1 AR080444 A1 AR 080444A1
Authority
AR
Argentina
Prior art keywords
heterocycle
aryl
alkyl
agent
inhibitor
Prior art date
Application number
ARP110100644A
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English (en)
Inventor
Philip Manton Brown
Joel Philip Freiman
David Reed Powell
Original Assignee
Lexicon Pharmaceuticals Inc
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 Lexicon Pharmaceuticals Inc filed Critical Lexicon Pharmaceuticals Inc
Publication of AR080444A1 publication Critical patent/AR080444A1/es

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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/70—Carbohydrates; Sugars; Derivatives thereof
    • A61K31/7028—Compounds having saccharide radicals attached to non-saccharide compounds by glycosidic linkages
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/13—Amines
    • A61K31/155—Amidines (), e.g. guanidine (H2N—C(=NH)—NH2), isourea (N=C(OH)—NH2), isothiourea (—N=C(SH)—NH2)
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic 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
    • A61K31/4985—Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring systems
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/04—Anorexiants; Antiobesity agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/06—Antihyperlipidemics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • 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
    • A61P9/12—Antihypertensives
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D309/00—Heterocyclic compounds containing six-membered rings having one oxygen atom as the only ring hetero atom, not condensed with other rings
    • C07D309/32—Heterocyclic compounds containing six-membered rings having one oxygen atom as the only ring hetero atom, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K2300/00—Mixtures or combinations of active ingredients, wherein at least one active ingredient is fully defined in groups A61K31/00 - A61K41/00

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Epidemiology (AREA)
  • Organic Chemistry (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Engineering & Computer Science (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Molecular Biology (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Emergency Medicine (AREA)
  • Endocrinology (AREA)
  • Child & Adolescent Psychology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Saccharide Compounds (AREA)
  • Pyrane Compounds (AREA)

Abstract

Métodos para mejorar la salud cardiovascular y/o metabolica de pacientes, en particular de aquellos que padecen de diabetes de Tipo 2, así como compuestos y composiciones farmacéuticas utiles en los mismos. Reivindicacion 1: Una dosis de 300 mg/día o menor (por ejemplo 250, 200, 150, 100 o 50 mg/día o menor) de un inhibidor dual SGLT1/2 de la formula (1) o una sal farmacéuticamente aceptable del mismo, para ser utilizada en una mejora de la salud cardiovascular o metabolica de un paciente diabético o pre-diabético, en donde cada R1A es, de manera independiente, hidrogeno, alquilo, arilo o heterociclo; cada R6 es, de manera independiente, hidrogeno, hidroxilo, amino, alquilo, arilo, ciano, halogeno, heteroalquilo, heterociclo, nitro, C:::CR6A, OR6A, SR6A, SOR6A, SO2R6A, C(O)R6A, CO2R6A, CO2H, CON(R6A)(R6A), CONH(R6A), CONH2, NHC(O)R6A, o NHSO2R6A; cada R6A es, de manera independiente, alquilo, arilo o heterociclo; cada R7 es, de manera independiente, hidrogeno, hidroxilo, amino, alquilo, arilo, ciano, halogeno, heteroalquilo, heterociclo, nitro, C:::CR7a, OR7A, SR7A, SOR7A, SO2R7A, C(O)R7A, CO2R7A, CO2H, CON(R7A)(R7A), CONH(R7A), CONH2, NHC(O)R7A o NHSO2R7A; cada R7A es, de manera independiente, alquilo, arilo o heterociclo; m es 1-4; n es 1-3; p es 0-2; y en donde, de manera opcional, cada alquilo, arilo, heteroalquilo o heterociclo esta sustituido con uno o mas de alcoxi, amino, ciano, halo, hidroxilo o nitro. Reivindicacion 8: El uso de la reivindicacion 1, en donde el inhibidor dual de SGLT1/2 es de la formula (2). Reivindicacion 9: El uso de la reivindicacion 8, en donde el inhibidor dual de SGLT1/2 es de la formula (3). Reivindicacion 10: El uso de la reivindicacion 9, en donde el inhibidor dual de SGLT1/2 es de la formula (4). Reivindicacion 13: El uso de la reivindicacion 12, en donde el inhibidor dual de SGLT1/2 es el (2S,3R,4R,5S,6R)-2-(4-cloro-3-(4-etoxibencil)fenilo)-6-(metiltio)tetrahidro-2H-piran-3,4,5-triol. Reivindicacion 14: El uso de la reivindicacion 1, en donde el paciente ha tomado, o está tomando de manera concurrente, un segundo agente terapéutico, en donde dicho segundo agente terapéutico es un agente anti-diabético, un agente anti-hiperglicémico, un agente hipolipidémico/un agente que disminuye los lípidos, agentes anti-obesidad, un agente anti-hipertensivo o un supresor del apetito.
ARP110100644A 2010-03-02 2011-03-02 Metodos para la utilizacion de cotransportadores de sodio-glucosa 1 y 2 AR080444A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US30959210P 2010-03-02 2010-03-02

Publications (1)

Publication Number Publication Date
AR080444A1 true AR080444A1 (es) 2012-04-11

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Family Applications (1)

Application Number Title Priority Date Filing Date
ARP110100644A AR080444A1 (es) 2010-03-02 2011-03-02 Metodos para la utilizacion de cotransportadores de sodio-glucosa 1 y 2

Country Status (24)

Country Link
US (3) US20110218159A1 (es)
EP (1) EP2542236B1 (es)
JP (2) JP6126383B2 (es)
KR (2) KR20130026422A (es)
CN (1) CN102821764A (es)
AR (1) AR080444A1 (es)
AU (1) AU2011223861B2 (es)
BR (1) BR112012021771B1 (es)
CA (1) CA2791300C (es)
CY (1) CY1118611T1 (es)
DK (1) DK2542236T3 (es)
ES (1) ES2609104T3 (es)
HR (1) HRP20170093T1 (es)
HU (1) HUE031441T2 (es)
IL (1) IL221372A0 (es)
LT (1) LT2542236T (es)
MX (1) MX342423B (es)
PL (1) PL2542236T3 (es)
PT (1) PT2542236T (es)
RS (1) RS55620B1 (es)
RU (1) RU2012141893A (es)
SI (1) SI2542236T1 (es)
TW (1) TWI562775B (es)
WO (1) WO2011109333A1 (es)

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