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AR076067A1 - Composiciones y metodos para modular la senda de senalizacion de wnt - Google Patents

Composiciones y metodos para modular la senda de senalizacion de wnt

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Publication number
AR076067A1
AR076067A1 ARP100100593A ARP100100593A AR076067A1 AR 076067 A1 AR076067 A1 AR 076067A1 AR P100100593 A ARP100100593 A AR P100100593A AR P100100593 A ARP100100593 A AR P100100593A AR 076067 A1 AR076067 A1 AR 076067A1
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AR
Argentina
Prior art keywords
carbon atoms
halogen
optionally substituted
alkoxy
alkyl
Prior art date
Application number
ARP100100593A
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English (en)
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Irm Llc
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Publication date
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First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=42112245&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=AR076067(A1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Irm Llc filed Critical Irm Llc
Publication of AR076067A1 publication Critical patent/AR076067A1/es

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    • AHUMAN NECESSITIES
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    • 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
    • A61K31/54Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one sulfur as the ring hetero atoms, e.g. sulthiame
    • A61K31/541Non-condensed thiazines containing further heterocyclic rings
    • AHUMAN NECESSITIES
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    • 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
    • A61K31/4427Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/4439Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
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    • 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
    • A61K31/4427Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/444Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring heteroatom, e.g. amrinone
    • 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
    • A61K31/496Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
    • 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
    • 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
    • A61K31/50Pyridazines; Hydrogenated pyridazines
    • A61K31/501Pyridazines; Hydrogenated pyridazines not condensed and containing further heterocyclic rings
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    • 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
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    • A61P13/00Drugs for disorders of the urinary system
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    • AHUMAN NECESSITIES
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    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D213/00Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/60Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D213/72Nitrogen atoms
    • C07D213/75Amino or imino radicals, acylated by carboxylic or carbonic acids, or by sulfur or nitrogen analogues thereof, e.g. carbamates
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    • 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
    • C07D401/02Heterocyclic 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 two hetero rings
    • C07D401/12Heterocyclic 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 two hetero rings linked by a chain containing hetero atoms as chain links
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    • C07D403/12Heterocyclic 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 linked by a chain containing hetero atoms as chain links
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    • 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

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Epidemiology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Immunology (AREA)
  • Hematology (AREA)
  • Biomedical Technology (AREA)
  • Rheumatology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Urology & Nephrology (AREA)
  • Neurosurgery (AREA)
  • Dermatology (AREA)
  • Diabetes (AREA)
  • Neurology (AREA)
  • Psychology (AREA)
  • Obesity (AREA)
  • Vascular Medicine (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Ophthalmology & Optometry (AREA)
  • Transplantation (AREA)
  • Oncology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Pyridine Compounds (AREA)
  • Steroid Compounds (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)

Abstract

Reivindicacion 1: Un compuesto que tiene la formula (1) o (2): o una sal fisiologicamente aceptable del mismo, en donde: el anillo E es un arilo o heteroarilo opcionalmente sustituido; A1 y A2 son independientemente un heterociclo de 1 a 5 átomos de carbono, quinolinilo, o un heteroarilo seleccionado a partir del grupo: (3) en donde cualquier heterociclo de A1 y A2 puede estar opcionalmente sustituido con -LC(O)R10; B es benzotiazolilo, quinolinilo o isoquinolinilo, cada uno de los cuales está opcionalmente sustituido con 1 a 3 grupos R6; X1, X2, X3 y X4 son independientemente CR7 o N; Y es fenilo o un heteroarilo de 5 a 6 miembros que contiene de 1 a 2 heteroátomos seleccionados a partir de N, O y S; Z es arilo, heterociclo de 1 a 5 átomos de carbono, o un heteroarilo de 5 a 6 miembros que contiene de 1 a 2 heteroátomos seleccionados a partir de N, O y S; cada Y y Z está opcionalmente sustituido con 1 a 3 grupos R6; R1 y R5 son independientemente H o alquilo de 1 a 6 átomos de carbono; R2 y R3 son independientemente H, alquilo de 1 a 6 átomos de carbono, o halogeno; R4 es halogeno, ciano, alcoxilo de 1 a 6 átomos de carbono, o un alquilo de 1 a 6 átomos de carbono opcionalmente sustituido con halogeno, alcoxilo o amino; R6 es hidrogeno, halogeno, alcoxilo de 1 a 6 átomos de carbono, -S(O)2R10, -C(O)OR10, -C(O)R10, -C(O)NR8R9, alquilo de 1 a 6 átomos de carbono, alquenilo de 2 a 6 átomos de carbono, o alquinilo de 2 a 6 átomos de carbono, cada uno de los cuales puede estar opcionalmente sustituido con halogeno, amino, hidroxilo, alcoxilo o ciano; halogeno, CN, -L-W, NR8R9, -L-C(O)R10, -L-C(O)OR10, -LC(O)NR8R9, OR10; -L-S(O)2R10 o -L-S(O)2NR8R9; R7 es H, halogeno, alcoxilo de 1 a 6 átomos de carbono, -L-S(O)2R10, alquilo de 1 a 6 átomos de carbono opcionalmente sustituido con halogeno, mino, hidroxilo, alcoxilo o ciano; NR8R9, -L-C(O)R10, -L-C(O)NR8R9, OR10 -L-S(O)2R10 o -L-S(O)2NR8R9; R8 y R9 son independientemente H, -L-W, o alquilo de 1 a 6 átomos de carbono, alquenilo de 2 a 6 átomos de carbono, o alquinilo de 2 a 6 átomos de carbono, cada uno de los cuales puede estar opcionalmente sustituido con halogeno, amino, hidroxilo, alcoxilo o ciano; o R8 y R9, junto con los átomos con los que están unidos, pueden formar un anillo; R10 es H, -L-W, o alquilo de 1 a 6 átomos de carbono, alquenilo de 2 a 6 átomos de carbono, o alquinilo de 2 a 6 átomos de carbono, cada uno de los cuales puede estar opcionalmente sustituido con halogeno, amino, hidroxilo, alcoxilo o ciano; L es un enlace o (CR2)1-4 en donde R es H o alquilo de 1 a 6 átomos de carbono; W es cicloalquilo de 3 a 7 átomos de carbono, heterociclo de 1 a 5 átomos de carbono, arilo o heteroarilo; m es de 0 a 4; n es de 0 a 3; y p es de 0 a 2.
ARP100100593A 2009-03-02 2010-03-01 Composiciones y metodos para modular la senda de senalizacion de wnt AR076067A1 (es)

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US15659909P 2009-03-02 2009-03-02
US24518709P 2009-09-23 2009-09-23

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AR076067A1 true AR076067A1 (es) 2011-05-18

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EP (2) EP2623493B1 (es)
JP (2) JP5490153B2 (es)
KR (1) KR101359873B1 (es)
CN (2) CN102731379B (es)
AR (1) AR076067A1 (es)
AU (1) AU2010221493C1 (es)
BR (1) BRPI1009235B8 (es)
CA (1) CA2753552C (es)
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UA103918C2 (en) * 2009-03-02 2013-12-10 Айерем Элелси N-(hetero)aryl, 2-(hetero)aryl-substituted acetamides for use as wnt signaling modulators
CA2756535A1 (en) 2009-03-23 2010-09-30 Glenmark Pharmaceuticals, S.A. Furopyrimidinedione derivatives as trpa1 modulators
CA2789189A1 (en) 2010-03-10 2011-09-15 Ingenium Pharmaceuticals Gmbh Inhibitors of protein kinases
UY33469A (es) 2010-06-29 2012-01-31 Irm Llc Y Novartis Ag Composiciones y metodos para modular la via de señalizacion de wnt
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