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AR082696A1 - Derivados heterociclicos nitrogenados de 1,2,4-oxadiazol, composiciones farmaceuticas que los contienen y uso de los mismos en el tratamiento de enfermedades cardiovasculares e inflamatorias, entre otras - Google Patents

Derivados heterociclicos nitrogenados de 1,2,4-oxadiazol, composiciones farmaceuticas que los contienen y uso de los mismos en el tratamiento de enfermedades cardiovasculares e inflamatorias, entre otras

Info

Publication number
AR082696A1
AR082696A1 ARP110102966A ARP110102966A AR082696A1 AR 082696 A1 AR082696 A1 AR 082696A1 AR P110102966 A ARP110102966 A AR P110102966A AR P110102966 A ARP110102966 A AR P110102966A AR 082696 A1 AR082696 A1 AR 082696A1
Authority
AR
Argentina
Prior art keywords
alkyl
optionally
substituted
membered
independently
Prior art date
Application number
ARP110102966A
Other languages
English (en)
Inventor
Heather Tye
Todd Bosanac
Alessandra Bartolozzi
Alan Olague
Doris Riether
Weimin Liu
Lifen Wu
Renee Zindell
Lombeart Stephane De
Tina M Morwick
Zhidong Chen
John D Huber
Ho Yin Lo
Pui Leng Loke
Original Assignee
Boehringer Ingelheim Int
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
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=44511591&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=AR082696(A1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Boehringer Ingelheim Int filed Critical Boehringer Ingelheim Int
Publication of AR082696A1 publication Critical patent/AR082696A1/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
    • 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
    • A61K31/4965Non-condensed pyrazines
    • A61K31/497Non-condensed pyrazines containing further heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • 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
    • 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
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • 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
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/08Antiallergic agents
    • 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
    • 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
    • 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
    • C07D413/02Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/10Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a carbon chain containing aromatic rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D417/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/14Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D471/00Heterocyclic 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
    • C07D471/02Heterocyclic 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
    • C07D471/04Ortho-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D498/00Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/02Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D498/04Ortho-condensed systems

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Engineering & Computer Science (AREA)
  • Cardiology (AREA)
  • Biomedical Technology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Pulmonology (AREA)
  • Urology & Nephrology (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Immunology (AREA)
  • Hospice & Palliative Care (AREA)
  • Rheumatology (AREA)
  • Pain & Pain Management (AREA)
  • Vascular Medicine (AREA)
  • Psychiatry (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)

Abstract

Reivindicación 1: Un compuesto caracterizado por la fórmula (1) en la que cada uno de R1 y R2 es independientemente hidrógeno, alquilo C1-7 o carbociclo C3-10, con la condición de que R1 y R2 no sean los dos hidrógeno; R3 es un anillo de heteroarilo de 5 - 11 miembros que contiene de uno a tres heteroátomos seleccionados entre nitrógeno, oxígeno y azufre, donde el anillo de heteroarilo está opcionalmente sustituido independientemente con uno a tres grupos seleccionados entre alquilo C1-5 opcionalmente sustituido con uno a tres átomos de halógeno, alcoxi C1-5, hidroxi C1-3, halógeno, hidroxi, -O-bencilo, oxo, ciano, amino, -NH-carbociclo C3-6, alquilamino C1-6 y dialquilamino C1-3; R4 es hidrógeno, alquilo C1-3, halógeno o nitrilo; R5 es alquilo C1-6, carbociclo C3-10, heterociclo de 3 - 11 miembros, arilo, heteroarilo de 5 - 11 miembros, -C(O)-R6, hidroxi o -NR7R8, donde cada R5 está opcionalmente sustituido independientemente con uno a tres grupos seleccionados entre R9, R10 y R11; R6 es heterociclo C3-8 o -NH-heterociclo de 5 - 6 miembros, cada uno opcionalmente sustituido independientemente con uno a tres grupos seleccionados entre R9, R10 y R11; cada uno de R7 y R8 es independientemente hidrógeno, heterociclo de 5 - 6 miembros opcionalmente sustituido con alquilo C1-6, carbociclo C3-10 opcionalmente sustituido con hidroxi o alquilo C1-6; R9, R10 y R11 se seleccionan independientemente entre (a) -H, (b) -OH, (c) halógeno, (d) -CN, (e) -CF3, (f) alquilo C1-6 opcionalmente sustituido con uno a tres -OH, -N(R12)(R13), heterociclo de 3 - 6 miembros, alcoxi C1-6, alcoxi C1-6-O-alquilo C1-6, -CO2R12, -C(O)N(R12)(R13) o -S(O)n-alquilo C1-6, (g) alcoxi C1-6, (h) -N(R12)(R13), (i) -S(O)n-alquilo C1-6, (j) -CO2R12, (k) -C(O)N(R12)(R13), (l) -S(O)2N(R12)(R13), (m) un grupo heterocíclico de 3 - 10 miembros opcionalmente sustituido con uno a tres grupos alquilo C1-6, (n) oxo, (o) -C(O)-alquilo C1-3; cada uno de R12 y R13 se selecciona independientemente entre -H, -alquilo C1-6, -C(O)alquilo C1-6, y un grupo heterocíclico de 3 - 6 miembros, cada uno de los cuales está opcionalmente sustituido independientemente con uno a tres grupos alquilo C1-6, -OH, alcoxi C1-6, -C(O)N(R14)(R15), -S(O)n-alquilo C1-6, CN, un grupo heterocíclico de 3 - 6 miembros, -O-alquilo C1-6, CF3; o R12 y R13 tomados junto con el anillo de nitrógeno al que están unidos forman un anillo de heterociclilo opcionalmente sustituido con uno a tres -OH, CN, -O-alquilo C1-6 u oxo; cada uno de R14 y R15 se selecciona independientemente entre -H y -alquilo C1-6; n es 0, 1 ó 2; o una sal farmacéuticamente aceptable del mismo.
ARP110102966A 2010-08-16 2011-08-15 Derivados heterociclicos nitrogenados de 1,2,4-oxadiazol, composiciones farmaceuticas que los contienen y uso de los mismos en el tratamiento de enfermedades cardiovasculares e inflamatorias, entre otras AR082696A1 (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US37392510P 2010-08-16 2010-08-16
US201161492176P 2011-06-01 2011-06-01

Publications (1)

Publication Number Publication Date
AR082696A1 true AR082696A1 (es) 2012-12-26

Family

ID=44511591

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP110102966A AR082696A1 (es) 2010-08-16 2011-08-15 Derivados heterociclicos nitrogenados de 1,2,4-oxadiazol, composiciones farmaceuticas que los contienen y uso de los mismos en el tratamiento de enfermedades cardiovasculares e inflamatorias, entre otras

Country Status (23)

Country Link
US (1) US8658661B2 (es)
EP (1) EP2606045B1 (es)
JP (1) JP5619284B2 (es)
KR (1) KR20130100105A (es)
CN (1) CN103180314A (es)
AP (1) AP2013006678A0 (es)
AR (1) AR082696A1 (es)
AU (1) AU2011292285A1 (es)
BR (1) BR112013003439A2 (es)
CA (1) CA2807364A1 (es)
CL (1) CL2013000455A1 (es)
CO (1) CO6680645A2 (es)
EA (1) EA201300250A1 (es)
EC (1) ECSP13012494A (es)
MX (1) MX2013001872A (es)
NZ (1) NZ605690A (es)
PE (1) PE20130751A1 (es)
PH (1) PH12013500301A1 (es)
SG (1) SG187549A1 (es)
TW (1) TW201238947A (es)
UY (1) UY33557A (es)
WO (1) WO2012024150A1 (es)
ZA (1) ZA201300238B (es)

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AP2013006678A0 (en) 2010-08-16 2013-01-31 Boehringer Ingelheim Int Oxadiazole inhibitors of leukotriene production
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US8580825B2 (en) * 2010-09-23 2013-11-12 Boehringer Ingelheim International Gmbh Oxadiazole inhibitors of leukotriene production
PH12013500545A1 (en) * 2010-09-23 2013-05-06 Boehringer Ingelheim Int Oxadiazole inhibitors of leukotriene production
US9073895B2 (en) * 2010-12-16 2015-07-07 Boehringer Ingelheim International Gmbh Biarylamide inhibitors of leukotriene production
WO2012129037A1 (en) 2011-03-18 2012-09-27 Boehringer Ingelheim International Gmbh Process for preparing carboxylic acids
US9174980B2 (en) * 2012-01-31 2015-11-03 Boehringer Ingelheim International Gmbh Heterocyclic compounds as inhibitors of leukotriene production
AR089853A1 (es) * 2012-02-01 2014-09-24 Boehringer Ingelheim Int Inhibidores de oxadiazol de la produccion de leucotrienos para terapia de combinacion, composicion farmaceutica, uso
US9029592B2 (en) * 2012-02-09 2015-05-12 Boehringer Ingelheim International Gmbh Process for preparing carboxamidine compounds
EP2746256A1 (en) 2012-12-19 2014-06-25 Basf Se Fungicidal imidazolyl and triazolyl compounds
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Also Published As

Publication number Publication date
CA2807364A1 (en) 2012-02-23
JP5619284B2 (ja) 2014-11-05
NZ605690A (en) 2014-06-27
EP2606045A1 (en) 2013-06-26
EP2606045B1 (en) 2016-01-06
PE20130751A1 (es) 2013-06-21
PH12013500301A1 (en) 2013-03-25
TW201238947A (en) 2012-10-01
SG187549A1 (en) 2013-03-28
CO6680645A2 (es) 2013-05-31
ECSP13012494A (es) 2013-04-30
US20120220561A1 (en) 2012-08-30
MX2013001872A (es) 2013-09-02
ZA201300238B (en) 2014-06-25
CN103180314A (zh) 2013-06-26
US8658661B2 (en) 2014-02-25
CL2013000455A1 (es) 2013-05-03
AU2011292285A1 (en) 2013-01-31
UY33557A (es) 2012-03-30
BR112013003439A2 (pt) 2019-09-24
JP2013534245A (ja) 2013-09-02
AP2013006678A0 (en) 2013-01-31
WO2012024150A1 (en) 2012-02-23
KR20130100105A (ko) 2013-09-09
EA201300250A1 (ru) 2013-08-30

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