AR079389A1 - GPR MODULATORS 119 - Google Patents

GPR MODULATORS 119

Info

Publication number
AR079389A1
AR079389A1 ARP100101569A ARP100101569A AR079389A1 AR 079389 A1 AR079389 A1 AR 079389A1 AR P100101569 A ARP100101569 A AR P100101569A AR P100101569 A ARP100101569 A AR P100101569A AR 079389 A1 AR079389 A1 AR 079389A1
Authority
AR
Argentina
Prior art keywords
alkyl
cycloalkyl
hydrogen
cyano
halogen
Prior art date
Application number
ARP100101569A
Other languages
Spanish (es)
Inventor
R Robinson
B Lefker
M Munchhof
E Darout
M Deninno
K Futatsugi
C Guimaraes
V Mascitti
K Mcclure
Original Assignee
Pfizer
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 Pfizer filed Critical Pfizer
Publication of AR079389A1 publication Critical patent/AR079389A1/en

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Classifications

    • 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
    • C07D401/14—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 three or more hetero rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
    • 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
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • A61P15/08—Drugs for genital or sexual disorders; Contraceptives for gonadal disorders or for enhancing fertility, e.g. inducers of ovulation or of spermatogenesis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • A61P15/10—Drugs for genital or sexual disorders; Contraceptives for impotence
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • A61P19/10—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease for osteoporosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/18—Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • 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
    • 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
    • A61P27/12—Ophthalmic agents for cataracts
    • 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
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A61P7/02—Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
    • 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
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
    • C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
    • C07D491/08—Bridged systems

Abstract

Composicion farmacéutica y sus usos en el tratamiento de enfermedades ligadas a la modulacion del receptor acoplado a proteína G GPR119 en animales. Reivindicacion 1: Un compuesto de la formula (1) caracterizado porque X es (2); R1 es -C(O)-O-R5 o (3); R2 es hidrogeno, ciano o metilo; R3 es hidrogeno, OH, halogeno, ciano, CF3, OCF3, alcoxi C1-5 o alquilo C1-5; R4 está ausente o es -CO-NR8R9, triazol, tetrazol, alquilo C1-5, NH2, -NH-alquilo C1-5, -N(CH3)-CO-O-alquilo C1-5, -NH-CO-alquilo C1-5 o -N(CH3)-CO-alquilo C1-5; R5 es alquilo C1-5, cicloalquilo C3-6 o cicloalquilo C3-6 en el que el átomo de carbono de dicho resto cicloalquilo está opcionalmente sustituido con metilo o etilo; R6 es CF3, alquilo C1-5, halogeno, ciano o cicloalquilo C3-6; R7 es cicloalquilo C3-6, alquilo C1-5, NH2 o -(CH2)2-OH; R8 es hidrogeno o alquilo C1-5, R9 es hidrogeno, alquilo C1-5, cicloalquilo C3-6, -CH2-CH2-OH, -CH2-CH2-O-CH3, -CH2-CH2-CH2-O-CH3, -CH2-CH2-CH2-OH, 3-oxetanilo o 3-hidroxiciclobutilo, R10 es hidrogeno, ciano, nitro, CF3, OCF3, cicloalquilo C3-6, alcoxi C1-5 o alquilo C1-5; R11 es hidrogeno, alquilo C1-5 o halogeno; y cada uno de A1, A2, A3 y A4 es independientemente CH, N-oxido o N; con la condicion de que: c) no más de 2 de A1, A2, A3 y A4 sean N; y d) no más de 1 de A1, A2, A3 y A4 sean N-oxido; o una sal farmacéuticamente aceptable del mismo.Pharmaceutical composition and its uses in the treatment of diseases linked to the modulation of the GPR119 G protein-coupled receptor in animals. Claim 1: A compound of the formula (1) characterized in that X is (2); R1 is -C (O) -O-R5 or (3); R2 is hydrogen, cyano or methyl; R3 is hydrogen, OH, halogen, cyano, CF3, OCF3, C1-5 alkoxy or C1-5 alkyl; R4 is absent or is -CO-NR8R9, triazole, tetrazole, C1-5 alkyl, NH2, -NH-C1-5 alkyl, -N (CH3) -CO-O-C1-5 alkyl, -NH-CO-alkyl C1-5 or -N (CH3) -CO-C1-5 alkyl; R5 is C1-5 alkyl, C3-6 cycloalkyl or C3-6 cycloalkyl wherein the carbon atom of said cycloalkyl moiety is optionally substituted with methyl or ethyl; R6 is CF3, C1-5 alkyl, halogen, cyano or C3-6 cycloalkyl; R7 is C3-6 cycloalkyl, C1-5 alkyl, NH2 or - (CH2) 2-OH; R8 is hydrogen or C1-5 alkyl, R9 is hydrogen, C1-5 alkyl, C3-6 cycloalkyl, -CH2-CH2-OH, -CH2-CH2-O-CH3, -CH2-CH2-CH2-O-CH3, -CH2-CH2-CH2-OH, 3-oxetanyl or 3-hydroxycyclobutyl, R10 is hydrogen, cyano, nitro, CF3, OCF3, C3-6 cycloalkyl, C1-5 alkoxy or C1-5 alkyl; R11 is hydrogen, C1-5 alkyl or halogen; and each of A1, A2, A3 and A4 is independently CH, N-oxide or N; with the proviso that: c) no more than 2 of A1, A2, A3 and A4 are N; and d) no more than 1 of A1, A2, A3 and A4 are N-oxide; or a pharmaceutically acceptable salt thereof.

ARP100101569A 2009-05-08 2010-05-07 GPR MODULATORS 119 AR079389A1 (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US17652809P 2009-05-08 2009-05-08
US32045710P 2010-04-02 2010-04-02

Publications (1)

Publication Number Publication Date
AR079389A1 true AR079389A1 (en) 2012-01-25

Family

ID=42813461

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP100101569A AR079389A1 (en) 2009-05-08 2010-05-07 GPR MODULATORS 119

Country Status (5)

Country Link
EP (1) EP2427450A1 (en)
JP (1) JP2012526097A (en)
AR (1) AR079389A1 (en)
CA (1) CA2759843A1 (en)
WO (1) WO2010128425A1 (en)

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EP2427450A1 (en) 2012-03-14
WO2010128425A1 (en) 2010-11-11
JP2012526097A (en) 2012-10-25
CA2759843A1 (en) 2010-11-10

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