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AR065453A1 - Producto farmaceutico y metodo de tratamiento - Google Patents

Producto farmaceutico y metodo de tratamiento

Info

Publication number
AR065453A1
AR065453A1 ARP080100757A ARP080100757A AR065453A1 AR 065453 A1 AR065453 A1 AR 065453A1 AR P080100757 A ARP080100757 A AR P080100757A AR P080100757 A ARP080100757 A AR P080100757A AR 065453 A1 AR065453 A1 AR 065453A1
Authority
AR
Argentina
Prior art keywords
chloro
spiro
benzofuran
piperidin
oxy
Prior art date
Application number
ARP080100757A
Other languages
English (en)
Inventor
Tomas Eriksson
Johan Hansson
John Mo
Marguerite Mensonides-Harsema
Original Assignee
Astrazeneca Ab
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 Astrazeneca Ab filed Critical Astrazeneca Ab
Publication of AR065453A1 publication Critical patent/AR065453A1/es

Links

Classifications

    • 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
    • A61K31/438The ring being spiro-condensed with carbocyclic or heterocyclic ring systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/56Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
    • A61K31/565Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids not substituted in position 17 beta by a carbon atom, e.g. estrane, estradiol
    • A61K31/568Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids not substituted in position 17 beta by a carbon atom, e.g. estrane, estradiol substituted in positions 10 and 13 by a chain having at least one carbon atom, e.g. androstanes, e.g. testosterone
    • A61K31/569Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids not substituted in position 17 beta by a carbon atom, e.g. estrane, estradiol substituted in positions 10 and 13 by a chain having at least one carbon atom, e.g. androstanes, e.g. testosterone substituted in position 17 alpha, e.g. ethisterone
    • 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
    • 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
    • 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
    • C07D471/10Spiro-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D491/00Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
    • C07D491/02Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
    • C07D491/10Spiro-condensed systems

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pulmonology (AREA)
  • Epidemiology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)

Abstract

Composiciones farmacéuticas y métodos para tratar enfermedades de las vías respiratorias, en especial una enfermedad pulmonar obstructiva cronica (COPD) y asma, en mamíferos por administracion de dicha combinacion Reivindicacion 1: Un productofarmacéutico caracterizado porque comprende, en combinacion, (a) un primer ingrediente activo, que consiste en un compuesto de formula general (1): donde: m es 0, 1 o 2; R1 es halogeno, ciano o haloalquilo C1-6; X, Y y Z son independientemente unaunion, -O-, -NH-, CH2- o -C(O)-, con la condicion de que solo uno de X, Y y Z es una union, y con la condicion de que X y Y no deben ser de manera simultánea -O- o -C(O)-; n es 0, 1 o 2; R2 es =O o alquilo C1-6; q es 0 o 1; R3 es hidrogeno,hidroxilo o NH2; R8 es hidrogeno o alquilo C1-6; A es una union o alquilo C1-3; R4 es hidrogeno, hidroxilo, oxo, NHC(O)R10, C(O)NR11R12, COOR13 o SO3R13 es hidrogeno, halogeno, hidroxilo o alcoxi C1-6, opcionalmente sustituido con uno o mássustituyentes que se seleccionan independientemente entre halogeno, ciano, hidroxilo y carboxilo; t es 0, 1 o 2; es halogeno, ciano, C1-3alcoxi o haloalquilo C1-3; R10 es hidrogeno, alquilo C1-3, NR11R12 o OR13; R11 y R12 se seleccionanindependientemente entre hidrogeno, alquilo y cicloalquilo C3-7, o R11 y R12 junto con el átomo de nitrogeno al que están unidos forman un anillo heterocíclico de entre 4 y 7 miembros, el cual se puede sustituir opcionalmente con uno o más gruposhidroxilo; y R13 es hidrogeno o alquilo C1-3, o una sal del mismo aceptable para uso farmacéutico; y (b) un segundo ingrediente activo, que es un agonista del receptor de glucocorticoide; y opcionalmente (c) un tercer ingrediente activo, queconsiste en a beta2-agonista, con la condicion de que el agonista no se seleccione entre una N-[2-(Dietilamino)etil]-N-(2-{[2-(4-hidroxi-2-oxo-2,3-dihidro-1,3-benzotiazol-7-il)etil]amino}etil)-3-[2-(1-naftil)etoxi]propanamida o una sal de la misma,a N-[2-(Dietilamino)etil]-N-(2-{[2-(4-hidroxi-2-oxo-2,3-dihidro-1,3-benzotiazol-7-il)etil]amino}etil)-3-[2-(3-clorofenil)etoxi]propanamida o una sal de la misma, o a 7-[(1R)-2-({2-[(3-{[2-(2-Clorofenil)etil]amino}propil)tio]etil}amino)-1-hidroxietil}-4-hidroxi-1,3-benzotiazol-2(3H)-ona o una sal de la misma. Reivindicacion 3: El producto farmacéutico de acuerdo con la reivindicacion 1, caracterizado porque el compuesto de formula (1) se selecciona entre: N-(2-{[(2S)-3-(5-cloro-1'H,3H-espiro[1-benzofuran-2,4'-piperidin]-1'-il)-2-hidroxipropil]oxi}-4-hidroxifenil)acetamida; Sal trifluoroacetato de N-(2-{[(2S)-3-(5-cloro-1'H-espiro[1,3-benzodioxol-2,4'-piperidin]-1'-il)-2-hidroxipropil]oxi}-4-hidroxifenil)acetamida; saltrifluoroacetato de 2-{[(2S)-3-(5-cloro-1'H,3H-espiro[1-benzofuran-2,4'-piperidin]-1'-il)-2-hidroxipropil]oxi}-4-hidroxi-N-metilbenzamida; sal trifluoroacetato del ácido 2-{[(2S)-3-(5-cloro-1'H,3H-espiro[1-benzofuran-2,4'-piperidin]-1'-il)-2-hidroxipropil]oxi}-4-hidroxibenzoico; Sal trifluoroacetato de N-(2-{[(2S)-3-(5-cloro-1'H,3H-espiro[2-benzofuran-1,4-piperidin]-1'-il)-2-hidroxipropil]oxi}-4-hidroxifenil)acetamida; 2-{[(2S)-3-(5-cloro-1'H,3H-espiro[2-benzofuran-1,4'-piperidin]-1'-il)-2-hidroxipropil]oxi}-4-hidroxi-N-metilbenzamida; N-(2-{[(2S)-3-(5-fluoro-1'H,3H-espiro[1-benzofuran-2,4-piperidin]-1'-il)-2-hidroxipropil]oxi}-4-hidroxifenil)acetamida; 2-{[(2S)-3-(5-fluoro-1'H,3H-espiro[1-benzofuran-2,4'-piperidin]-1'-il)-2-hidroxipropil}oxi}-4-hidroxi-N-metilbenzamida; N-[2-({(2S)-3-[(2R)-5-cloro-1'H,3H-espiro[1-benzofuran-2,3-pirrolidin]-1'-il]-2-hidroxipropil}oxi-4-hidroxifenil]acetamida; Sal trifluoroacetato de N-(2-{[(2S)-3-(5-cloro-1'H,3H-espiro[1-benzofuran-2,4'-piperidin]-1'-il)-2-hidroxipropil]oxi}-4-hidroxifenil)urea; clorhidrato del ácido 4-fluoro-2-{[(2S)-3-(5-fluoro-1'H,3H-espiro[1-benzofuran-2,4'-piperidin]-1'-il)-2-hidroxipropil]oxi}benzoico; Sal trifluoroacetato de N-(2-{[(2S)-3-(5-cloro-1'H,3H-espiro[1-benzofuran-2,4'- piperidin]-1'-il)-2-hidroxipropil]oxi}-4-fluorofenil)urea; Sal bis(trifluoroacetato) de N-(2-{[(2S)-2-amino-3-(5-fluoro-1'H,3H-espiro[1-benzofuran-2,4'-piperidin]-1'-iI)propil]oxi}-4-hidroxifenil)acetamida; 2-[(2S)-3-(5-clorospiro[benzofuran-2(3H),4'-piperidin]-1'-il)-2-hidroxipropoxi]-benzaldehido; Espiro[benzofuran-2(3H),4'-piperidin]-1'-etanol, 5-cloro-alfa-[[2-(2-hidroxietil)fenoxi]metil]-, (alfaS)-; Espiro[benzofuran-2(3H),4'-piperidin]-1'-etanol, 5-cloro-alfa-[[2-(hidroximetil)fenoxi]metil]-, (alfaS)-; N-(2-{[(2S)-3-(5-cloro-1'H,3H-espiro[1-benzofuran-2,4'-piperidin]-1'-il)-2-hidroxipropil]oxi}-5-cloro-4-hidroxifenil)acetamida; ácido 2-Cloro-5-{[(2S)-3-(5-cloro-1'H,3H-espiro[1-benzofuran-2,4'-piperidin]-1'-iI)-2-hidroxipropil)oxi}-(4-{acetilamino}fenoxi)acético; ácido 5-{[(2S)-3-(5-Cloro-1'H,3H-espiro[1-benzofuran-2,4'-piperidin]-1'-il)-2-hidroxipropil]oxi}-(4-{acetilamino}fenoxi)acético; ácido {2-Cloro-5-{[(2S)-3-(5-cloro-1'H,3H-espiro[1-benzofuran-2,4'-piperidin]-1'-iI)-2-hidroxipropil]oxi}-4-[(metilamino)carbonil]fenoxi}acético; ácido 2-{2-Cloro-5-{((2S)-3-(5-cloro-1'H,3H-espiro[1-benzofuran-2,4'-piperidin]-1'-iI)-2-hidroxipropil]oxi}-4-[(metilamino)carbonil]fenoxi}-2-metilpropanoico; ácido (2-Cloro-5-{[(2S)-3-(5-cloro-1'H,3H-espiro[1-benzofuran-2,4'-piperidin]-1'-iI)-2-hidroxipropil]oxi}-4-{[(3S)-3-hidroxipirrolidin-1-iI]carbonil}fenoxi)acético; sal trifluoroacetato del ácido 5-Cloro-2-{[(2S)-3-(S-cloro-1'H,3H-espiro[1-benzofuran-2,4'-piperidin]-1'-il)-2-hidroxipropil]oxi}-4-(cianometoxi)benzoico; sal trifluoroacetato del ácido 2-{[(2S)-3-(5-cloro-1'H,3H-espiro[1-benzofuran-2,4'-piperidin]-1'-il)-2-hidroxipropil]oxi}-5-cloro-4-(2,2-difluoroetoxi)benzoico;sal trifluoroacetato del ácido 5-Cloro-2-{[(2S)-3-(5-cloro-1'H,3H-espiro[1-benzofuran-2,4'-piperidin]-1'-iI)-2-hidroxipropil]oxi}-4-(3,3,3-trifluoropropoxi)benzoico; Sal trifluoroacetato de N-(2-{3-[5-cloro-1'H,3H-espiro[1-benzofuran-2,4'-piperidin]-1'-il]propoxi}fenil)acetamida; Sal de ácido trifluoroacético y ácido metil 3-(2-{[(2S)-3-(5-cloro-1'H3H-espiro[1-benzofuran-2,4'-piperidin]-1'-il)-2-hidroxipropil]oxi}-4-fluorofenil) propanoico; N-(2-{[(2S)-3-({espiro[indol-2,4'-piperidin]-3(1H)-ona}-1'-il)-2-hidroxipropil]oxi}-4-hidroxifenil)acetamida; y ácido (2-{[(2S)-3-(5-Cloro-1'H,3H-espiro[1-benzofuran-2,4'-piperidin]-1'-il)-2-hidroxipropil]oxi}-4-fluorofenil)metansulfonico o una sal aceptable para su uso farmacéutico, un solvato osal solvatada del mismo. Reivindicacion 5: El producto farmacéutico de acuerdo con cualquiera de las reivindicaciones precedentes, caracterizado porque el agonista del receptor de glucocorticoide es budesonida. Reivindicacion 6: El productofarmacéutico de acuerdo con cualquiera de las reivindicaciones precedentes, caracterizado porque el beta2-agonista se selecciona entre cualquiera entre formoterol, indacaterol o una N-[2-(Dietilamino)etil]-N-(2-{[2-(4-hidroxi-2-oxo-2,3-dihidro-1,3-benzotiazol-7-il)etil]amino}etil)-3-[2-(1-naftiI)etoxi]propanamida o una sal de la misma, una N-[2-(Dietilamino)etil]-N-(2-{[2-(4-hidroxi-2-oxo-2,3-dihidro-1,3-benzotiazol-7-iI)etil]amino}etil)-3-[2-(3-clorofenil)etoxi]propanamida o una sal de lamisma, o una 7-[(1R)-2-({2-[(3-{[2-(2-Clorofenil)etil]amino}propil)tio]etil}amino)-1-hidroxietil]-4-hidroxi-1,3-benzotiazol-2(3H)-ona o una sal de la misma.
ARP080100757A 2007-02-23 2008-02-22 Producto farmaceutico y metodo de tratamiento AR065453A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US89124407P 2007-02-23 2007-02-23

Publications (1)

Publication Number Publication Date
AR065453A1 true AR065453A1 (es) 2009-06-10

Family

ID=39710315

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP080100757A AR065453A1 (es) 2007-02-23 2008-02-22 Producto farmaceutico y metodo de tratamiento

Country Status (8)

Country Link
US (1) US20110124613A1 (es)
EP (1) EP2120935A4 (es)
AR (1) AR065453A1 (es)
CL (1) CL2008000539A1 (es)
PE (1) PE20090491A1 (es)
TW (1) TW200848035A (es)
UY (1) UY30935A1 (es)
WO (1) WO2008103126A1 (es)

Families Citing this family (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2009543860A (ja) * 2006-07-19 2009-12-10 アストラゼネカ・アクチエボラーグ 新規三環系スピロピペリジン化合物、それらの合成およびケモカイン受容体活性モジュレーターとしてのそれらの使用
UY32521A (es) * 2009-04-03 2010-10-29 Astrazeneca Ab Combinación para emplear en el tratamiento de enfermedades respiratorias
WO2012163848A1 (en) 2011-05-27 2012-12-06 INSERM (Institut National de la Santé et de la Recherche Médicale) Methods and pharmaceutical compositions for the treatment of crohn's disease
EP2771484A1 (en) 2011-10-28 2014-09-03 Galderma Research & Development New leukocyte infiltrate markers for rosacea and uses thereof
WO2016100940A1 (en) 2014-12-19 2016-06-23 The Broad Institute, Inc. Dopamine d2 receptor ligands
WO2016100823A1 (en) 2014-12-19 2016-06-23 The Broad Institute, Inc. Dopamine d2 receptor ligands
GB201918692D0 (en) 2019-12-18 2020-01-29 Cambridge Entpr Ltd Treatment and prognosis of pancreatic cancer

Family Cites Families (9)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB2373186A (en) * 2001-02-23 2002-09-18 Astrazeneca Ab Pharmaceutical combinations of a CCR3 antagonist and a compound which is usefulreatment of asthma, allergic disease or inflammation
GB0207436D0 (en) * 2002-03-28 2002-05-08 Glaxo Group Ltd Novel compounds
SE0202133D0 (sv) * 2002-07-08 2002-07-08 Astrazeneca Ab Novel compounds
SE0303090D0 (sv) * 2003-11-20 2003-11-20 Astrazeneca Ab Novel compounds
SE0303280D0 (sv) * 2003-12-05 2003-12-05 Astrazeneca Ab Novel compounds
SE0303541D0 (sv) * 2003-12-22 2003-12-22 Astrazeneca Ab New compounds
TW200744612A (en) * 2005-08-26 2007-12-16 Astrazeneca Ab New combination
AU2006282122A1 (en) * 2005-08-26 2007-03-01 Astrazeneca Ab A combination of compounds, which can be used in the treatment of respiratory diseases, especially chronic obstructive pulmonary disease (COPD) and asthma
JP2009543860A (ja) * 2006-07-19 2009-12-10 アストラゼネカ・アクチエボラーグ 新規三環系スピロピペリジン化合物、それらの合成およびケモカイン受容体活性モジュレーターとしてのそれらの使用

Also Published As

Publication number Publication date
UY30935A1 (es) 2008-09-30
EP2120935A1 (en) 2009-11-25
EP2120935A4 (en) 2011-06-22
US20110124613A1 (en) 2011-05-26
PE20090491A1 (es) 2009-05-31
WO2008103126A1 (en) 2008-08-28
CL2008000539A1 (es) 2008-10-10
TW200848035A (en) 2008-12-16

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