AR061858A1 - Compuestos heterociclicos de fosfonatos y fosfinatos, composiciones farmaceuticas que los contienen y usos como agentes antidiabeticos. - Google Patents

Compuestos heterociclicos de fosfonatos y fosfinatos, composiciones farmaceuticas que los contienen y usos como agentes antidiabeticos.

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Publication number
AR061858A1
AR061858A1 ARP070103051A ARP070103051A AR061858A1 AR 061858 A1 AR061858 A1 AR 061858A1 AR P070103051 A ARP070103051 A AR P070103051A AR P070103051 A ARP070103051 A AR P070103051A AR 061858 A1 AR061858 A1 AR 061858A1
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AR
Argentina
Prior art keywords
group
heteroaryl
hydrogen
aryl
alkyl
Prior art date
Application number
ARP070103051A
Other languages
English (en)
Inventor
Denis E Ryono
Wei Meng
Joseph A Tino
Scott A Bolton
Sean Chen
Yan Shi
Hao Zhang
Peter T W Cheng
Richard B Sulsky
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Bristol Myers Squibb Co
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Application filed by Bristol Myers Squibb Co filed Critical Bristol Myers Squibb Co
Publication of AR061858A1 publication Critical patent/AR061858A1/es

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    • C07F9/00Compounds containing elements of Groups 5 or 15 of the Periodic Table
    • C07F9/02Phosphorus compounds
    • C07F9/547Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
    • C07F9/6536Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having nitrogen and sulfur atoms with or without oxygen atoms, as the only ring hetero atoms
    • C07F9/6539Five-membered rings
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    • C07ORGANIC CHEMISTRY
    • C07FACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F9/00Compounds containing elements of Groups 5 or 15 of the Periodic Table
    • C07F9/02Phosphorus compounds
    • C07F9/28Phosphorus compounds with one or more P—C bonds
    • C07F9/30Phosphinic acids [R2P(=O)(OH)]; Thiophosphinic acids ; [R2P(=X1)(X2H) (X1, X2 are each independently O, S or Se)]
    • C07F9/32Esters thereof
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/66Phosphorus compounds
    • A61K31/675Phosphorus compounds having nitrogen as a ring hetero atom, e.g. pyridoxal phosphate
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
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    • A61P19/00Drugs for skeletal disorders
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    • A61P19/00Drugs for skeletal disorders
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    • A61P27/00Drugs for disorders of the senses
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    • A61P27/06Antiglaucoma agents or miotics
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    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/04Anorexiants; Antiobesity agents
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    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/06Antihyperlipidemics
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    • A61P3/00Drugs for disorders of the metabolism
    • 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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    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/04Inotropic agents, i.e. stimulants of cardiac contraction; Drugs for heart failure
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    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/10Drugs 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P9/12Antihypertensives
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    • C07F9/00Compounds containing elements of Groups 5 or 15 of the Periodic Table
    • C07F9/02Phosphorus compounds
    • C07F9/28Phosphorus compounds with one or more P—C bonds
    • C07F9/38Phosphonic acids [RP(=O)(OH)2]; Thiophosphonic acids ; [RP(=X1)(X2H)2(X1, X2 are each independently O, S or Se)]
    • C07F9/40Esters thereof
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    • C07FACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F9/00Compounds containing elements of Groups 5 or 15 of the Periodic Table
    • C07F9/02Phosphorus compounds
    • C07F9/547Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
    • C07F9/553Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having one nitrogen atom as the only ring hetero atom
    • C07F9/576Six-membered rings
    • C07F9/58Pyridine rings
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    • C07F9/00Compounds containing elements of Groups 5 or 15 of the Periodic Table
    • C07F9/02Phosphorus compounds
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    • C07F9/645Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having two nitrogen atoms as the only ring hetero atoms
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    • C07F9/65031Five-membered rings having the nitrogen atoms in the positions 1 and 2
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    • C07F9/00Compounds containing elements of Groups 5 or 15 of the Periodic Table
    • C07F9/02Phosphorus compounds
    • C07F9/547Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
    • C07F9/645Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having two nitrogen atoms as the only ring hetero atoms
    • C07F9/6509Six-membered rings
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    • C07F9/00Compounds containing elements of Groups 5 or 15 of the Periodic Table
    • C07F9/02Phosphorus compounds
    • C07F9/547Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
    • C07F9/6515Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having three nitrogen atoms as the only ring hetero atoms
    • C07F9/6518Five-membered rings

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
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  • Pharmacology & Pharmacy (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Engineering & Computer Science (AREA)
  • Molecular Biology (AREA)
  • Biochemistry (AREA)
  • Diabetes (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Obesity (AREA)
  • Hematology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Biomedical Technology (AREA)
  • Ophthalmology & Optometry (AREA)
  • Neurosurgery (AREA)
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Abstract

Reivindicacion 1: Un compuesto caracterizado porque tiene la estructura (1) en donde R1 es un heteroarilo substituido por R4 y substituido opcionalmente con uno o dos substituyentes R5 y R6, en donde el heteroarilo posee un átomo de nitrogeno adyacente al átomo que une el grupo heteroarilo a -NH-C(=O); R4 se selecciona del grupo que consiste de -(CH2)n-Z-(CH2)m-PO(OR7)(OR8), o -(CH2)nZ- (CH2)m-PO(OR7)R9, o -(CH2)n-Z(CH2)m-O-PO(OR7)R9, o -(CH2)nZ-(CH2)m-O-PO(R9)R10 o -(CH2)nZ-(CH2)m- PO(R9)R10; R7 y R8 son iguales o diferentes y se seleccionan independientemente del grupo que consiste de hidrogeno y alquilo, o R7 y R8 pueden ciclizarse en un anillo de formula (2) donde q = 1-3; R9 y R10 son iguales o diferentes y se seleccionan independientemente del grupo que consiste de alquilo, arilo, arilalquilo, heteroarilo y heteroarilalquilo; o R9 y R10 pueden ciclizarse en un anillo de formula (3) o (4) donde q = 1-3 o R7 y R9 pueden ciclizarse en un anillo de formula (5) o (6) donde q =1-3; Z se selecciona de un enlace, alquileno, alquenileno, O, S o SO2; m es 0,1 o 2, con la condicion de que cuando Z es O, S o SO2, m es 1 o 2; n es 0, 1 o 2; R5 y R6 son iguales o diferentes y se seleccionan independientemente del grupo que consiste de hidrogeno, alquilo, halogeno, o carboxilo, o está ausente; X se selecciona del grupo que consiste de formulas (7) y un enlace X-6; y cuando Y está ausente, X es como en formulas (8); R2 se selecciona del grupo que consiste de hidrogeno, alquilo, cicloalquilo, heterociclilo, arilo, heteroarilo, alquinilo, y alquenilo; p es 0 o 1; Q se selecciona del grupo que consiste de O, S(O)q y CO, donde q es 0, 1 o 2; Q1 se selecciona del grupo que consiste de hidrogeno y fluor; R11 se selecciona del grupo que consiste de hidrogeno, alquilo inferior, cicloalquilo, arilo y heteroarilo; R12 se selecciona del grupo que consiste de hidrogeno, y alquilo inferior, o R11 y R12 juntos con el átomo de carbono al cual se enlazan, forman un anillo de cicloalquilo de 5 hasta 7 átomos de carbono; R13 se selecciona del grupo que consiste de halo, nitro, amino, ciano, metilo, trifluorometilo, hidroxi, metoxi, trifluorometoxi, metiltio, metilsulfinilo o metilsulfonilo; T se selecciona del grupo que consiste de arilo y heteroarilo; Y es R3-(CH2)s-, o está ausente; R3 se selecciona del grupo que consiste de arilo o heteroarilo; s = 0 o 1; todos los estereoisomeros del mismo, un éster de profármaco del mismo o una sal farmacéuticamente aceptable del mismo.
ARP070103051A 2006-07-06 2007-07-06 Compuestos heterociclicos de fosfonatos y fosfinatos, composiciones farmaceuticas que los contienen y usos como agentes antidiabeticos. AR061858A1 (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US81891206P 2006-07-06 2006-07-06
US11/769,964 US7910747B2 (en) 2006-07-06 2007-06-28 Phosphonate and phosphinate pyrazolylamide glucokinase activators

Publications (1)

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AR061858A1 true AR061858A1 (es) 2008-09-24

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ARP070103051A AR061858A1 (es) 2006-07-06 2007-07-06 Compuestos heterociclicos de fosfonatos y fosfinatos, composiciones farmaceuticas que los contienen y usos como agentes antidiabeticos.

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US (3) US7910747B2 (es)
EP (1) EP2059522B1 (es)
JP (3) JP5361714B2 (es)
KR (1) KR101375406B1 (es)
AR (1) AR061858A1 (es)
AU (1) AU2007269171B2 (es)
BR (1) BRPI0713929A2 (es)
CA (1) CA2658001C (es)
CL (1) CL2007001994A1 (es)
CO (1) CO6390122A2 (es)
EA (1) EA015228B1 (es)
ES (1) ES2449572T3 (es)
IL (1) IL196226A (es)
MX (1) MX2008016514A (es)
NO (1) NO20085160L (es)
NZ (1) NZ573734A (es)
PE (1) PE20081001A1 (es)
SG (1) SG173358A1 (es)
TW (1) TWI418558B (es)
WO (1) WO2008005964A2 (es)

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