AR081197A1 - Lactamas sustituidas con piperidinil o como moduladores de gpr 119 - Google Patents

Lactamas sustituidas con piperidinil o como moduladores de gpr 119

Info

Publication number
AR081197A1
AR081197A1 ARP110101683A ARP110101683A AR081197A1 AR 081197 A1 AR081197 A1 AR 081197A1 AR P110101683 A ARP110101683 A AR P110101683A AR P110101683 A ARP110101683 A AR P110101683A AR 081197 A1 AR081197 A1 AR 081197A1
Authority
AR
Argentina
Prior art keywords
alkyl
optionally substituted
alkoxy
halogen
methyl
Prior art date
Application number
ARP110101683A
Other languages
English (en)
Inventor
Ajay Singh
Kevin Ronald Condroski
Scott Alan Pratt
Thomas Daniel Aicher
Josef Roland Bencsik
Ronald Jay Hinklin
John Peter Fischer
Timothy M Turner
Jay Bradford Fell
Steven Armen Boyd
Original Assignee
Array Biopharma 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 Array Biopharma Inc filed Critical Array Biopharma Inc
Publication of AR081197A1 publication Critical patent/AR081197A1/es

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D413/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • 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
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445Non condensed piperidines, e.g. piperocaine
    • A61K31/4523Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/4545Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. pipamperone, anabasine
    • 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
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/18Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/28Drugs 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/04Anorexiants; Antiobesity agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/06Antihyperlipidemics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • 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
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/12Antihypertensives
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic 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
    • C07D401/14Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D405/00Heterocyclic 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
    • C07D405/14Heterocyclic 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 three or more hetero rings

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Diabetes (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Obesity (AREA)
  • Hematology (AREA)
  • Biomedical Technology (AREA)
  • Psychiatry (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Emergency Medicine (AREA)
  • Vascular Medicine (AREA)
  • Urology & Nephrology (AREA)
  • Endocrinology (AREA)
  • Immunology (AREA)
  • Child & Adolescent Psychology (AREA)
  • Hospice & Palliative Care (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Low-Molecular Organic Synthesis Reactions Using Catalysts (AREA)

Abstract

Son moduladores de GPR119 y son útiles en el tratamiento o la prevención de enfermedades tales como, en forma no taxativa, diabetes tipo 2, complicaciones diabéticas, síntomas de la diabetes, síndrome metabólico, obesidad, dislipidemia y condiciones relacionadas. Reivindicación 1: Un compuesto caracterizado porque tiene la fórmula general (1 ) o una sal farmacéuticamente aceptable o un solvato de él, en donde L es O o NRx; Rx es H o alquilo C1-3; X1 es N o CR1 y X2 es N o CR2, en donde solamente uno de X1 y X2 puede ser N; R1, R2, R3 y R4 se seleccionan independientemente de H, halógeno, CF3, alquilo C1-6 y alcoxi C1-6; R5 es alquilo C1-3sulfonilo, cicloalquilo C3-6 sulfonilo, (ciclopropilmetil)sulfonilo, fenilsulfonilo, CN, Br, CF3, triazolilo, alcoxi C1-4carbonilo, RxRyNHC(=O)-, oxadiazolilo opcionalmente sustituido con alquilo C1-3, y tetrazolilo opcionalmente sustituido con alquilo C1-3; o cuando X1 es CR1 y X2 es CR2, entonces R4 y R5 opcionalmente junto con los átomos a los cuales están unidos forman un anillo heterocíclico saturado de 5-6 miembros que tiene 1-2 heteroátomos del anillo seleccionados independientemente de O y S y opcionalmente sustituidos con un grupo oxo, en donde el S cuando está presente está opcionalmente oxidado; Rx y Ry son independientemente alquilo C1-4) opcionalmente sustituido con OH, o Rx y Ry junto con el átomo al cual están unidos forman un anillo azacíclico saturado de 5-6 miembros opcionalmente sustituidos con OH; R6 es H, OH o metilo; R6a es H o metilo; R7 es un grupo que tiene la estructura de fórmulas (2); A1 es N o CRa; A2 es N o CRb; A3 es N o CRc; A4 es N o CRd, en donde por lo menos uno de A1, A2, A3 y A4 es N, y no más de dos de A1, A2, A3 y A4 pueden ser N; Ra, Rb, Rc y Rd son independientemente H, CF3, halógeno, alquilo C1-4 o CN; R8 se selecciona de hidrógeno, halógeno CF3, CN, alquilo C1-10, hidroxialquilo C1-6, alcoxi C1-6, alquilo C1-6sulfanilo, fenilo, piridilo, pirimidilo, pirazolilo, y dialquilo C1-3carbamilo, en donde cada uno de dichos fenilo, piridilo, pirimidilo, y pirazolilo se sustituye opcionalmente con uno o más sustituyentes seleccionados independientemente de alquilo C1-4, alcoxi C1-4 y CF3; R9 y R9a son independientemente hidrógeno o metilo; y n es 1, 2 o 3.
ARP110101683A 2010-05-17 2011-05-17 Lactamas sustituidas con piperidinil o como moduladores de gpr 119 AR081197A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US34546110P 2010-05-17 2010-05-17

Publications (1)

Publication Number Publication Date
AR081197A1 true AR081197A1 (es) 2012-07-04

Family

ID=44584599

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP110101683A AR081197A1 (es) 2010-05-17 2011-05-17 Lactamas sustituidas con piperidinil o como moduladores de gpr 119

Country Status (20)

Country Link
US (1) US8754226B2 (es)
EP (1) EP2571864A1 (es)
JP (1) JP2013530947A (es)
KR (1) KR20130113948A (es)
CN (1) CN103080101A (es)
AR (1) AR081197A1 (es)
AU (1) AU2011256455A1 (es)
BR (1) BR112012029395A2 (es)
CA (1) CA2799779A1 (es)
CL (1) CL2012003211A1 (es)
CO (1) CO6670520A2 (es)
CR (1) CR20120642A (es)
IL (1) IL223092A0 (es)
MX (1) MX2012013465A (es)
RU (1) RU2012154308A (es)
SG (1) SG185615A1 (es)
TW (1) TW201141849A (es)
UY (1) UY33392A (es)
WO (1) WO2011146335A1 (es)
ZA (1) ZA201209605B (es)

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EP2872127A1 (en) 2012-07-11 2015-05-20 Elcelyx Therapeutics, Inc. Compositions comprising statins, biguanides and further agents for reducing cardiometabolic risk
US9499482B2 (en) 2012-09-05 2016-11-22 Bristol-Myers Squibb Company Pyrrolone or pyrrolidinone melanin concentrating hormone receptor-1 antagonists
AR092924A1 (es) 2012-10-09 2015-05-06 Sanofi Sa Derivados de pirrolidinona como moduladores de gpr119 para el tratamiento de diabetes, obesidad, dislipidemia y trastornos relacionados
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AR099937A1 (es) 2014-04-04 2016-08-31 Sanofi Sa Compuestos de isoindolinona como moduladores de gpr119 para el tratamiento de diabetes, obesidad, dislipidemia y trastornos relacionados
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Also Published As

Publication number Publication date
EP2571864A1 (en) 2013-03-27
RU2012154308A (ru) 2014-06-27
US20130158009A1 (en) 2013-06-20
WO2011146335A1 (en) 2011-11-24
US8754226B2 (en) 2014-06-17
CL2012003211A1 (es) 2013-04-26
AU2011256455A1 (en) 2013-01-10
MX2012013465A (es) 2013-12-02
TW201141849A (en) 2011-12-01
CA2799779A1 (en) 2011-11-24
ZA201209605B (en) 2014-05-28
BR112012029395A2 (pt) 2016-07-26
IL223092A0 (en) 2013-02-03
SG185615A1 (en) 2012-12-28
KR20130113948A (ko) 2013-10-16
UY33392A (es) 2012-11-30
CO6670520A2 (es) 2013-05-15
CN103080101A (zh) 2013-05-01
CR20120642A (es) 2013-03-11
JP2013530947A (ja) 2013-08-01

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