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AR098622A1 - Derivados de benzhidrilo - Google Patents

Derivados de benzhidrilo

Info

Publication number
AR098622A1
AR098622A1 ARP140104521A ARP140104521A AR098622A1 AR 098622 A1 AR098622 A1 AR 098622A1 AR P140104521 A ARP140104521 A AR P140104521A AR P140104521 A ARP140104521 A AR P140104521A AR 098622 A1 AR098622 A1 AR 098622A1
Authority
AR
Argentina
Prior art keywords
alkyl
group
hydrogen
integer
range
Prior art date
Application number
ARP140104521A
Other languages
English (en)
Inventor
Capaldi Carmelid
Riccaboni Mauro
Van De Pol Herv
De Fanti Renato
Armani Elisabetta
Amari Gabriele
Baker-Glenn Charles
Original Assignee
Chiesi Farm Spa
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 Chiesi Farm Spa filed Critical Chiesi Farm Spa
Publication of AR098622A1 publication Critical patent/AR098622A1/es

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D453/00—Heterocyclic compounds containing quinuclidine or iso-quinuclidine ring systems, e.g. quinine alkaloids
    • C07D453/02—Heterocyclic compounds containing quinuclidine or iso-quinuclidine ring systems, e.g. quinine alkaloids containing not further condensed quinuclidine ring systems
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic 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
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/444—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring heteroatom, e.g. amrinone
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic 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
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445—Non condensed piperidines, e.g. piperocaine
    • A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/4545—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. pipamperone, anabasine
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic 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
    • A61K31/496—Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/0012—Galenical forms characterised by the site of application
    • A61K9/007—Pulmonary tract; Aromatherapy
    • A61K9/0073—Sprays or powders for inhalation; Aerolised or nebulised preparations generated by other means than thermal energy
    • A61K9/0075—Sprays or powders for inhalation; Aerolised or nebulised preparations generated by other means than thermal energy for inhalation via a dry powder inhaler [DPI], e.g. comprising micronized drug mixed with lactose carrier particles
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic 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
    • C07D401/02—Heterocyclic 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
    • C07D401/12—Heterocyclic 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic 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
    • C07D401/14—Heterocyclic 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 three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic 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
    • C07D405/14—Heterocyclic 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14—Heterocyclic 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic 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
    • C07D417/14—Heterocyclic 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

Landscapes

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

Abstract

Compuestos con una estructura de benzhidrilo que pueden actuar como inhibidores de la enzima fosfodiesterasa 4 (PDE4) y también como antagonistas de los receptores muscarínicos M3, con métodos para prepararlos, con composiciones que los comprenden y con su uso en terapia, en el tratamiento de la enfermedad pulmonar obstructiva crónica (EPOC). Reivindicación 1: Un compuesto caracterizado porque es de fórmula general (1) donde cada R¹ es hidrógeno o se selecciona entre el grupo que consiste en: halógeno, C₁₋₄ alquilo, C₁₋₄ alcoxi, C₁₋₄ haloalquilo, hidroxi, -SO₂NR⁶R⁷, -CN, -NR⁸SO₂R⁹, -NR⁶R⁷, -CONR⁶R⁷ y -NR⁸COR⁹ y donde dicho C₁₋₄ alquilo está opcionalmente sustituido con uno o más grupos seleccionados entre C₃₋₇ cicloalquilo, hidroxi y -NR⁶R⁷ y donde dicho C₁₋₄ alcoxi está opcionalmente sustituido con uno o más halógenos o grupos C₃₋₇ cicloalquilo donde, R⁶ es hidrógeno o C₁₋₆ alquilo; R⁷ es hidrógeno o C₁₋₆ alquilo; R⁸ es hidrógeno o C₁₋₆ alquilo; R⁹ es hidrógeno o C₁₋₆ alquilo; n es un entero en el rango entre 1 y 3; cada R² es hidrógeno o se selecciona entre el grupo que consiste en: halógeno, C₁₋₄ alquilo, C₁₋₄ alcoxi, C₁₋₄ haloalquilo, hidroxi, -SO₂NR¹⁰R¹¹, -CN y -NR¹²SO₂R¹³ y donde dicho C₁₋₄ alquilo y dicho C₁₋₄ alcoxi están opcionalmente sustituidos con un grupo C₃₋₇ cicloalquilo, donde R¹⁰ es hidrógeno o C₁₋₆ alquilo; R¹¹ es hidrógeno o C₁₋₆ alquilo; R¹² es hidrógeno o C₁₋₆ alquilo; R¹³ es hidrógeno o C₁₋₆ alquilo; m es un entero en el rango entre 1 y 3; R³ y R⁴ son diferentes o iguales y se seleccionan en forma independiente entre el grupo que consiste en: H; C₃₋₇ cicloalquilcarbonilo; C₁₋₆ alquilo, opcionalmente sustituido con uno o más sustituyentes seleccionados entre C₃₋₇ cicloalquilo o C₅₋₇ cicloalquenilo; C₁₋₆ haloalquilo; C₃₋₇ cicloalquilo; C₅₋₇ cicloalquenilo; C₂₋₆ alquenilo; y C₂₋₆ alquinilo; o R³ y R⁴, junto con los átomos que los interconectan, forman un anillo 2,2-difluoro-1,3-dioxolano de fórmula (2) fusionado a la unidad fenilo que se une a los grupos -OR³ y -OR⁴, donde los asteriscos indican átomos de carbono compartidos con dicho anillo fenilo; cada R⁵ se selecciona entre el grupo que consiste en: CN, NO₂, CF₃ y átomos de halógeno; k es 0 o un entero en el rango entre 1 y 3; L¹ se selecciona entre la lista que consiste en: un enlace, -(CH₂)ₚ-, [3]-(CH₂)ₚ-O-[4], [3]-(CH₂)ₚ-NR¹⁰-(CH₂)ₜ-[4], [3]-(CH₂)ₚ-OC(O)-[4], [3]-(CH₂)ₚ-NR¹⁰C(O)-[4], [3]-(CH₂)ₚ-NR¹⁰-S(O₂)-[4] y [3]-(CH₂)ₚ-S(O₂)-N(R¹⁰)-[4] donde [3] y [4] representan, respectivamente, el punto de unión del grupo L¹ al grupo carbonilo y al anillo W y donde R¹⁰ es como se describe precedentemente, p es un entero en el rango entre 1 y 4 y t es un entero en el rango entre 1 y 4; W es un grupo divalente seleccionado entre arileno, C₅₋₆ heteroarileno y C₃₋₇ heterocicloalquileno monocíclico saturado; L² es una unión o es un grupo seleccionado entre -C(O)-, -S-, -S(O)-, -S(O)₂- y -(CH₂)q- donde q es 1 ó 2; L³ se encuentra ausente o se selecciona entre orto-, meta-, para-fenileno, y un C₅₋₆ heteroarileno bivalente; L⁴ es un grupo seleccionado entre -(CH₂)ʳ-, [1]-(CH₂)ʳ-O-[2], [1]-OC(O)-[2] y [1]-C(O)O-[2] donde r es 1 ó 2 y [1] y [2] representan respectivamente el punto de unión del grupo L⁴ al grupo L² y al anillo fenilo; Z se selecciona entre NH, CH₂ y O; A es un grupo que contiene nitrógeno que puede seleccionarse entre: un grupo (a) que es -(CH₂)ₛ-NR¹⁶R¹¹ donde s es un entero en el rango entre 1 y 4 y R¹⁶ y R¹⁷ son en forma independiente hidrógeno o C₁₋₄ alquilo; y un grupo (b) que es un sistema de anillos heterocíclico monocíclico, bicíclico o tricíclico saturado opcionalmente sustituido con uno o dos grupos R¹⁸ que se seleccionan en forma independiente entre si entre C₁₋₄ alquilo y bencilo; N-óxido en el anillo piridina, derivado deuterado y sal o solvato farmacéuticamente aceptable del mismo.
ARP140104521A 2013-12-05 2014-12-04 Derivados de benzhidrilo AR098622A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
EP13195932 2013-12-05

Publications (1)

Publication Number Publication Date
AR098622A1 true AR098622A1 (es) 2016-06-01

Family

ID=49726581

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP140104521A AR098622A1 (es) 2013-12-05 2014-12-04 Derivados de benzhidrilo

Country Status (9)

Country Link
US (1) US9145409B2 (es)
EP (1) EP3077386B1 (es)
KR (1) KR20160085350A (es)
CN (1) CN105814034A (es)
AR (1) AR098622A1 (es)
CA (1) CA2932486A1 (es)
HK (1) HK1225384A1 (es)
RU (1) RU2016121852A (es)
WO (1) WO2015082619A1 (es)

Families Citing this family (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US9763924B2 (en) 2014-06-05 2017-09-19 Chiesi Farmaceutici S.P.A. Aminoester derivatives
US9326976B2 (en) 2014-06-05 2016-05-03 Chiesi Farmaceutici S.P.A. Carbamate derivatives
MA42048A (fr) 2015-05-07 2018-03-14 Chiesi Farm Spa Dérivés d'aminoesters
AR104822A1 (es) 2015-06-01 2017-08-16 Chiesi Farm Spa Derivado de aminoésteres
AR104829A1 (es) 2015-06-01 2017-08-16 Chiesi Farm Spa Derivados de aminoésteres

Family Cites Families (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP2022783A1 (en) 2007-08-08 2009-02-11 CHIESI FARMACEUTICI S.p.A. "Derivatives of 1-phenyl-2-pyridinyl alkyl alcohols as phosphodiesterase inhibitors"
EP2216327A1 (en) 2009-02-06 2010-08-11 CHIESI FARMACEUTICI S.p.A. Benzoic acid (1-phenyl-2-pyridin-4-yl)ethyl esters as phosphodiesterase inhibitors
EP2386555A1 (en) 2010-05-13 2011-11-16 Almirall, S.A. New cyclohexylamine derivatives having beta2 adrenergic agonist and m3 muscarinic antagonist activities
HK1198251A1 (en) * 2011-10-21 2015-03-20 奇斯药制品公司 Derivatives of 1-phenyl-2-pyridinyl alkyl alcohols as phosphodiesterase inhibitors
RU2015121044A (ru) 2012-12-05 2017-01-12 КЬЕЗИ ФАРМАЧЕУТИЧИ С.п.А. Производные фенилэтилпиридина в качестве ингибиторов pde4
TW201439089A (zh) 2012-12-05 2014-10-16 Chiesi Farma Spa 新穎化合物
AR093798A1 (es) 2012-12-05 2015-06-24 Chiesi Farm Spa Compuestos

Also Published As

Publication number Publication date
WO2015082619A1 (en) 2015-06-11
EP3077386B1 (en) 2017-09-06
US9145409B2 (en) 2015-09-29
HK1225384A1 (zh) 2017-09-08
RU2016121852A (ru) 2017-12-07
US20150158857A1 (en) 2015-06-11
CA2932486A1 (en) 2015-06-11
CN105814034A (zh) 2016-07-27
EP3077386A1 (en) 2016-10-12
KR20160085350A (ko) 2016-07-15

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