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AR061653A1 - Compuestos inhibidores de gsk3(glucogeno sintasa quinasa 3) - Google Patents

Compuestos inhibidores de gsk3(glucogeno sintasa quinasa 3)

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Publication number
AR061653A1
AR061653A1 ARP070102832A ARP070102832A AR061653A1 AR 061653 A1 AR061653 A1 AR 061653A1 AR P070102832 A ARP070102832 A AR P070102832A AR P070102832 A ARP070102832 A AR P070102832A AR 061653 A1 AR061653 A1 AR 061653A1
Authority
AR
Argentina
Prior art keywords
alkyl
heterocyclyl
optionally substituted
carbocyclyl
carbamoyl
Prior art date
Application number
ARP070102832A
Other languages
English (en)
Original Assignee
Astrazeneca Ab
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Publication date
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=38846128&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=AR061653(A1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Astrazeneca Ab filed Critical Astrazeneca Ab
Publication of AR061653A1 publication Critical patent/AR061653A1/es

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/14Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 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
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/506Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • A61P17/14Drugs for dermatological disorders for baldness or alopecia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • A61P19/08Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • A61P19/08Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • A61P19/10Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease for osteoporosis
    • 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
    • A61P25/14Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/14Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • A61P25/16Anti-Parkinson drugs
    • 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
    • A61P25/24Antidepressants
    • 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
    • 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
    • A61P35/00Antineoplastic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/04Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • 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

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Veterinary Medicine (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Rheumatology (AREA)
  • Diabetes (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Psychiatry (AREA)
  • Pain & Pain Management (AREA)
  • Psychology (AREA)
  • Endocrinology (AREA)
  • Obesity (AREA)
  • Hospice & Palliative Care (AREA)
  • Hematology (AREA)
  • Emergency Medicine (AREA)
  • Dermatology (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)

Abstract

La presente también se refiere a formulaciones farmacéuticas que contienen dicho compuesto y al uso de dicho compuesto en terapia, para trastornos cognitivos, diabetes, osteoporosis. La presente se refiere además a un proceso para la preparacion del compuesto de formula (1). Reivindicacion 1: Un compuesto de formula (1), donde A es heterociclilo o carbociclilo; donde dicho heterociclilo o carbociclilo está opcionalmente sustituido en carbono con uno o más R1 y donde si dicho heterociclilo contiene una porcion -NH-, ese nitrogeno puede estar opcionalmente sustituido con un grupo -R5-R7, con la salvedad de que dicho carbociclilo no es fenilo; R1 se selecciona entre halo, nitro, ciano, hidroxi, amino, sulfamoilo, carbamoilo, alquilo C1- 3, un carbociclilo, un heterociclilo y un grupo -R6-R7, donde dicho alquilo C1-3 está opcionalmente sustituido con uno o más halo y donde dicho carbociclilo o heterociclilo opcionalmente forma un sistema anular conjugado junto con A; R2 se selecciona entre halo, nitro, trifluorometilo, trifluorometoxi y ciano; R3 se seleccione entre metilo, alquilo C6, alquenilo C6, alquinilo C6, un carbociclilo no aromático de 6 miembros y un heterociclilo no aromático de 6 miembros, donde dicho alquilo C6, alquenilo C6, alquinilo C6, carbociclilo o heterociclilo está opcionalmente sustituido con uno o más halo, cieno, trifluorometoxi, haloalquilo C1-3 o alquilo C1-3; R4 se selecciona entre hidrogeno, alquilo C1-3, ciano y haloalquilo C1-3, donde dicho alquilo C1-3 o haloalquilo C1-3 está opcionalmente sustituido con uno o más OR8; donde R8 se selecciona independientemente entre hidrogeno, alquilo C1-6 o haloalquilo C1-6; R5 se selecciona entre -C(O)N(R9)-, -S(O)z-, -SO2N(R10)-, -SO2O- , -C(O)-, -C(O)O y (-CH2-)m; donde R9 y R10 se seleccionan independientemente entre hidrogeno o alquilo C1-6 y donde dicho alquilo C1-6 está opcionalmente sustituido con uno o más R19; y donde m es 0, 1, 2 o 3 y donde z es 1 o 2; R6 se selecciona entre -O-, -N(R11)C(O)-, -C(O)N(R12)-, -S(O)r-, -SO2N(R13)-, -N(R14)SO2-, -(CH2)pN(R15)-, -OSO2-, -C(O)-, -C(O)O-, -N(R16)C(O)O-, -N(R17)C(O)N(R18)- y (-CH2-)n; donde R11, R12, R13, R14, R15, R16, R17 y R18 se seleccionan independientemente entre hidrogeno o alquilo C1-6 y donde dicho alquilo C1-6 está opcionalmente sustituido con uno o más R19; y donde n es 0, 1, 2 o 3 y donde p es 0, 1, 2 o 3 y donde r es 0, 1 o 2; R7 se selecciona entre hidrogeno, alquilo C1-6, alquenilo C2-6, alquinilo C2-6, -alquil C1-4carbociclilo, -alquil C1-4heterociclilo, carbociclilo y heterociclilo; donde R7 puede estar opcionalmente sustituido en carbono con uno o más R20; y donde si dicho heterociclilo contiene una porcion -NH-, ese nitrogeno puede estar opcionalmente sustituido con un grupo seleccionado entre R21; R19 y R20 se seleccionan independientemente entre halo, nitro, ciano, hidroxi, amino, carboxi, carbamoilo, sulfamoilo, alquilo C1-6, alquenilo C2-6, alquinilo C2-6, alcoxi C1-6, alcoxi C1- 6-alcoxi C1-6, alcanoílo C1-6, N-(alquil C1-6)amino, N,N-(alquil C1-6)2amino, alcanoilamino C1-6, N-(alquil C1-6)carbamoilo, N,N(alquil C1-6)2carbamoílo, alquil C1-6S(O)a, alcoxi C1-6carbonilo, N(alquil C1-6)sulfamoilo, N,N-(alquil C1-6)2sulfamollo, alquil C1-6sulfonilamino, carbociclilo, heterociclilo, carbociclilalquil C1-6-R22-, heterociclilalquil C1-6-R23-, carbociclil-R24- y heterociclil-R25-; donde a es 0, 1 o 2; y donde R19 y R20 independientemente uno del otro, está opcionalmente sustituido en carbono con uno o más R26; y donde si dicho heterociclilo contiene una porcion -NH-, ese nitrogeno está opcionalmente sustituido con un grupo seleccionado entre R27; R22, R23, R24 y R25 se seleccionan independientemente entre -O-, - N(R28)-, -C(O)-, -N(R29)C(O)-, -C(O)N(R30)-, -S(O)s-, -SO2N(R31)- y -N(R32)SO2-; donde R28, R29, R30, R31 y R32 se seleccionan independientemente entre hidrogeno o alquilo C1-6 y s es 0, 1 o 2; R21 y R27 se seleccionan independientemente entre alquilo C1-6, alcanoílo C1-6, alquil C1-6sulfonilo, alcoxi C1-6carbonilo, carbamoilo, N-(alquil C1-6)carbamoilo, N,N-(alquil C1-6)carbamoilo, carbociclilo, heterociclilo, -alquil C1-6carbociclilo, -alquil C1-6heterociclilo, benciloxicarbonilo, benzoilo y fenilsulfonilo; donde R21 y R27 independientemente uno del otro, están opcionalmente sustituido en carbono con uno o más R33; y R26 y R33 se seleccionan independientemente entre halo, nitro, ciano, -alquil C1-3hidroxi, -alquil C1-3metoxi, -alquil C1-3etoxi, -alquil C1-3isopropoxi, hidroxi, trifluorometoxi, trifluorometilo, amino, carboxi, carbamoilo, mercapto, sulfamoilo, metilo, etilo, ciclopropilo, ciclobutilo, metoxi, etoxi, acetilo, acetoxi, metilamino, etilamino, dimetilamino, dietilamino, N-metil-N-etilamino, acetilamino, N-metilcarbamoilo, N-etilcarbamoilo, N,N-dimetilcarbamoilo, N,N-dietilcarbamoilo, N-metil-N-etilcarbamoilo, metiltio, etiltio, metilsulfinilo, etilsulfinilo, mesilo, etilsulfonilo, metoxicarbonilo, etoxicarbonilo, N-metilsulfamoilo, N-etilsulfamoilo, N,N-dimetilsulfamoilo, N,N-dietilsulfamoilo, N-metil-N-etilsulfamoilo, carbociclo y heterociclo; donde dicho carbociclo o heterociclo está opcionalmente sustituido con halo, metilo, trifluorometilo, ciano o etilo; como una base libre o una sal farmacéuticamente aceptable del mismo.
ARP070102832A 2006-06-27 2007-06-26 Compuestos inhibidores de gsk3(glucogeno sintasa quinasa 3) AR061653A1 (es)

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US (1) US20080188503A1 (es)
EP (1) EP2046783A4 (es)
JP (1) JP2009542639A (es)
KR (1) KR20090024295A (es)
CN (1) CN101511824A (es)
AR (1) AR061653A1 (es)
AU (1) AU2007265732A1 (es)
BR (1) BRPI0713578A2 (es)
CA (1) CA2655444A1 (es)
CL (1) CL2007001882A1 (es)
EC (1) ECSP088974A (es)
IL (1) IL195665A0 (es)
MX (1) MX2008015721A (es)
NO (1) NO20090328L (es)
RU (1) RU2008148903A (es)
TW (1) TW200815417A (es)
UY (1) UY30438A1 (es)
WO (1) WO2008002245A2 (es)
ZA (1) ZA200810577B (es)

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CN101511824A (zh) 2009-08-19
US20080188503A1 (en) 2008-08-07
TW200815417A (en) 2008-04-01
IL195665A0 (en) 2009-09-01
AU2007265732A1 (en) 2008-01-03
WO2008002245A2 (en) 2008-01-03
KR20090024295A (ko) 2009-03-06
NO20090328L (no) 2009-01-26
ZA200810577B (en) 2009-08-26
UY30438A1 (es) 2008-01-31
BRPI0713578A2 (pt) 2012-10-23
ECSP088974A (es) 2009-01-30
CL2007001882A1 (es) 2008-02-08
WO2008002245A3 (en) 2008-02-14
CA2655444A1 (en) 2008-01-03
MX2008015721A (es) 2009-01-08
JP2009542639A (ja) 2009-12-03
WO2008002245A8 (en) 2008-10-09
EP2046783A4 (en) 2010-08-04
EP2046783A2 (en) 2009-04-15
RU2008148903A (ru) 2010-08-10

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