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AR073209A1 - Tienopirimidinas utiles para la profilaxis y/o tratamiento de enfermedades influenciadas por la inhibicion de quinasas mnk1 y/o mnk2 ,tales como enfermedades metabolicas y trastornos inflamatorios,y composiciones farmaceuticas que las contienen. - Google Patents

Tienopirimidinas utiles para la profilaxis y/o tratamiento de enfermedades influenciadas por la inhibicion de quinasas mnk1 y/o mnk2 ,tales como enfermedades metabolicas y trastornos inflamatorios,y composiciones farmaceuticas que las contienen.

Info

Publication number
AR073209A1
AR073209A1 ARP090103272A ARP090103272A AR073209A1 AR 073209 A1 AR073209 A1 AR 073209A1 AR P090103272 A ARP090103272 A AR P090103272A AR P090103272 A ARP090103272 A AR P090103272A AR 073209 A1 AR073209 A1 AR 073209A1
Authority
AR
Argentina
Prior art keywords
alkyl
optionally substituted
heteroatom selected
heterocyclyl
heteroaryl
Prior art date
Application number
ARP090103272A
Other languages
English (en)
Inventor
John Danilewicz
Martin Schneider
Matthias Austen
Phillip Black
Ian Linney
Kay Schreiter
Wesley Blackaby
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=40266066&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=AR073209(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 AR073209A1 publication Critical patent/AR073209A1/es

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D495/00Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
    • C07D495/02Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D495/04Ortho-condensed systems
    • 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
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with 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
    • A61P11/06Antiasthmatics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • A61P11/08Bronchodilators
    • 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
    • A61P19/00Drugs for skeletal disorders
    • A61P19/06Antigout agents, e.g. antihyperuricemic or uricosuric agents
    • 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
    • A61P25/28Drugs 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
    • A61P3/00Drugs for disorders of the metabolism
    • 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
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/04Antibacterial agents
    • 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
    • A61P37/02Immunomodulators
    • A61P37/06Immunosuppressants, e.g. drugs for graft rejection
    • 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
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    • A61P7/00Drugs for disorders of the blood or the extracellular fluid
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P7/00Drugs for disorders of the blood or the extracellular fluid
    • A61P7/02Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
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    • A61P7/00Drugs for disorders of the blood or the extracellular fluid
    • A61P7/10Antioedematous agents; Diuretics
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    • 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
    • A61P9/12Antihypertensives

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Immunology (AREA)
  • Neurology (AREA)
  • Pulmonology (AREA)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Cardiology (AREA)
  • Rheumatology (AREA)
  • Pain & Pain Management (AREA)
  • Transplantation (AREA)
  • Hospice & Palliative Care (AREA)
  • Oncology (AREA)
  • Psychiatry (AREA)
  • Communicable Diseases (AREA)
  • Endocrinology (AREA)
  • Child & Adolescent Psychology (AREA)
  • Emergency Medicine (AREA)
  • Urology & Nephrology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)

Abstract

Reivindicacion 1: Un compuesto caracterizado porque tiene la formula general (1) en la que X se selecciona entre CH o N; R2 se selecciona entre H, CN, CF3, CON(R4)2; O-alquilo C1-8 opcionalmente sustituido con R3; heterociclilo C3-10 que comprende al menos un heteroátomo seleccionado entre N, S y O; heteroarilo C5-10 que comprende al menos un heteroátomo seleccionado entre N, S y O; y alquilo C1-8 opcionalmente sustituido con R6; y cuando X es CH, R2 también puede ser F, CI, SO2NH2; Y se selecciona entre alquilo C1-8 de cadena lineal o ramificada, opcionalmente sustituido con uno o más de R3; cicloalquilo C3-8, opcionalmente sustituido con uno o más de R9; y sistemas heterocíclicos seleccionados entre una cualquiera de las formulas (2) opcionalmente sustituido con uno o más de R9, donde n es independientemente 1 a 3 U es independientemente O o NR5; R1 se selecciona entre H; CI; y alquilo C1-8, opcionalmente sustituido con N(R4)2 o F; R3 se selecciona entre OH, OR4 y N(R4)2 desde el segundo átomo de carbono de la cadena alquilo al que se une R3 en adelante; F; CO2H; CON(R4)2; SO2N(R4)2; heterociclilo C3-10 que comprende al menos un heteroátomo seleccionado entre N, S y O donde el átomo de nitrogeno puede estar sustituido con H o alquilo C1-3; y heteroarilo C5-10 que comprende al menos un heteroátomo seleccionado entre N, S y O; R4 se selecciona entre H y alquilo C1-8; R5 se selecciona entre H; alquilo C1-8, alquenilo C2-8, cicloalquilo C3 -10; heterociclilo C3-10 que comprende al menos un heteroátomo seleccionado entre N, S y O; heteroarilo C5-10 que comprende al menos un heteroátomo seleccionada entre N, S y O; COR6, CO2R4; CONH(CH2)mR6; (CH2)mR6; CO(CH2)mR6; (CH2)mC(O)R6; SO2R4; y SO2(CH2)mR6; donde m es 1-4; R6 se selecciona entre H; OH; OR4; OC(O)R4; N(R4)2; F; CO2H; CON(R4)2; SO2N(R4)2; heterociclilo que comprende al menos un heteroátomo seleccionado entre N, S y O; y heteroarilo C5-10 que comprende al menos un heteroátomo seleccionado entre N, S y O y que está opcionalmente sustituido con alquilo C1-3 o N(R4)2; W se selecciona entre F; CI; Br; I; CN; -(CH2)1-2NR7R8; -C(S)NH2; -CONR7R8; -C(=NR7)NR7R8; -CO2R7; y -SO2NR7R8; o W junto con R1 puede formar un anillo heterocíclico de cinco o siete miembros que comprende al menos un heteroátomo seleccionado entre N, S y O, donde el átomo de nitrogeno puede estar sustituido con H, -C(O)-O-alquilo C1-4, -CO-(CH2)1-2-NH2, -CO-(CH2)1-2-NH(alquilo C1-3) o -CO-(CH2)1-2-N(alquilo C1-3)2; R7se selecciona entre H y alquilo C1-8; R8 se selecciona entre H; alquilo C1-8 opcionalmente sustituido con R3; heterociclilo C3-10 que comprende al menos un heteroátomo seleccionado entre N, S y O, opcionalmente sustituido con alquilo C1-3, y heteroarilo C5-10 que comprende al menos un heteroátomo seleccionado entre N, S y O; R9 se selecciona entre OH, OR4, N(R4)2, N(R4)COR4, NR4SO2R4 y N(R4)-(CH2)m-R4 sobre cualquier átomo de carbono distinto del unido a O o N; F; CO2H; CON(R4)2; SO2N(R4)2; SO2R4; (CH2)mOR4; (CH2)mN(R4)2; heterociclilo C3-10 que comprende al menos un heteroátomo seleccionado entre N, S y O y heteroarilo C5-10 que comprende al menos un heteroátomo seleccionado entre N, S y O; con la condicion de que se excluya el compuesto 4-(2-metoxifenilamino)-5-metiltieno[2,3-d]pirimidina-6-carboxilato de etilo; o un tautomero, metabolito, profármaco o una al farmacéuticamente aceptable del mismo.
ARP090103272A 2008-08-26 2009-08-25 Tienopirimidinas utiles para la profilaxis y/o tratamiento de enfermedades influenciadas por la inhibicion de quinasas mnk1 y/o mnk2 ,tales como enfermedades metabolicas y trastornos inflamatorios,y composiciones farmaceuticas que las contienen. AR073209A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
EP08015049 2008-08-26

Publications (1)

Publication Number Publication Date
AR073209A1 true AR073209A1 (es) 2010-10-20

Family

ID=40266066

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP090103272A AR073209A1 (es) 2008-08-26 2009-08-25 Tienopirimidinas utiles para la profilaxis y/o tratamiento de enfermedades influenciadas por la inhibicion de quinasas mnk1 y/o mnk2 ,tales como enfermedades metabolicas y trastornos inflamatorios,y composiciones farmaceuticas que las contienen.

Country Status (18)

Country Link
US (1) US8486953B2 (es)
EP (1) EP2331551B1 (es)
JP (1) JP5675614B2 (es)
KR (1) KR20110045019A (es)
CN (1) CN102186857A (es)
AR (1) AR073209A1 (es)
AU (1) AU2009286734A1 (es)
BR (1) BRPI0918971A2 (es)
CA (1) CA2735361A1 (es)
CL (1) CL2011000409A1 (es)
ES (1) ES2593495T3 (es)
IL (1) IL211008A0 (es)
MX (1) MX2011001938A (es)
NZ (1) NZ591113A (es)
RU (1) RU2011110908A (es)
TW (1) TW201014864A (es)
UY (1) UY32072A (es)
WO (1) WO2010023181A1 (es)

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KR20110045019A (ko) 2011-05-03
ES2593495T3 (es) 2016-12-09
TW201014864A (en) 2010-04-16
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WO2010023181A1 (en) 2010-03-04
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MX2011001938A (es) 2011-03-29
UY32072A (es) 2010-03-26
CA2735361A1 (en) 2010-03-04
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BRPI0918971A2 (pt) 2015-12-01
US20120128686A1 (en) 2012-05-24
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AU2009286734A1 (en) 2010-03-04
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