AR098621A1 - Derivados de heteroarilo - Google Patents

Derivados de heteroarilo

Info

Publication number
AR098621A1
AR098621A1 ARP140104520A ARP140104520A AR098621A1 AR 098621 A1 AR098621 A1 AR 098621A1 AR P140104520 A ARP140104520 A AR P140104520A AR P140104520 A ARP140104520 A AR P140104520A AR 098621 A1 AR098621 A1 AR 098621A1
Authority
AR
Argentina
Prior art keywords
alkyl
group
hydrogen
integer
range
Prior art date
Application number
ARP140104520A
Other languages
English (en)
Inventor
Van De Pol Herv
Whittaker Ben
Ghidini Eleonora
Amari Gabriele
Baker-Glenn Charles
Armani Elisabetta
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 AR098621A1 publication Critical patent/AR098621A1/es

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Classifications

    • 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
    • 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
    • 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
    • A61K31/4436—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a heterocyclic ring having sulfur as a ring hetero atom
    • 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
    • A61K31/4439—Non 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
    • 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
    • A61M—DEVICES FOR INTRODUCING MEDIA INTO, OR ONTO, THE BODY; DEVICES FOR TRANSDUCING BODY MEDIA OR FOR TAKING MEDIA FROM THE BODY; DEVICES FOR PRODUCING OR ENDING SLEEP OR STUPOR
    • A61M15/00—Inhalators
    • A61M15/0065—Inhalators with dosage or measuring devices
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61M—DEVICES FOR INTRODUCING MEDIA INTO, OR ONTO, THE BODY; DEVICES FOR TRANSDUCING BODY MEDIA OR FOR TAKING MEDIA FROM THE BODY; DEVICES FOR PRODUCING OR ENDING SLEEP OR STUPOR
    • A61M16/00—Devices for influencing the respiratory system of patients by gas treatment, e.g. mouth-to-mouth respiration; Tracheal tubes
    • A61M16/10—Preparation of respiratory gases or vapours
    • A61M16/14—Preparation of respiratory gases or vapours by mixing different fluids, one of them being in a liquid phase
    • 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
    • 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
    • A61P11/08—Bronchodilators
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61M—DEVICES FOR INTRODUCING MEDIA INTO, OR ONTO, THE BODY; DEVICES FOR TRANSDUCING BODY MEDIA OR FOR TAKING MEDIA FROM THE BODY; DEVICES FOR PRODUCING OR ENDING SLEEP OR STUPOR
    • A61M2202/00—Special media to be introduced, removed or treated
    • A61M2202/06—Solids
    • A61M2202/064—Powder

Landscapes

  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Engineering & Computer Science (AREA)
  • Pulmonology (AREA)
  • Anesthesiology (AREA)
  • Biomedical Technology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Hematology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Biophysics (AREA)
  • Emergency Medicine (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 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. Reivindicación 1: Un compuesto caracterizado porque es de fórmula general (1) donde cada R¹ es hidrógeno o se selecciona en forma independiente 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 uno o más grupos 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, cuando está presente, se selecciona en forma independiente 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-NR¹⁰S(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 W¹ 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; W¹ se selecciona entre un grupo C₅₋₆ heteroarileno divalente; W² se selecciona entre un arilo y un heteroarilo; L² es un grupo seleccionado entre -(CH₂)q- donde q es 1 ó 2; L³ es una unión o un grupo seleccionado entre -(CH₂)ₛ- donde s es 1 ó 2, X se selecciona entre N y [1]-N(R¹⁹)-CH<[2] donde [1] representa el punto de unión del grupo X a L² y [2] representa el punto de unión del grupo X al grupo W² y al grupo L³-C(O)OA y donde R¹⁹ se selecciona entre hidrógeno, C₁₋₆ alquilo y bencilo o, cuando W² es un anillo fenilo, R¹⁹ es opcionalmente un C₁₋₆ alquileno conectado a W² en posición orto con respecto a X, de manera de formar con W² y junto con los átomos que los interconectan un anillo condensado de la fórmula (3) donde la línea ondulada indica un punto de unión al resto de la molécula; A se selecciona entre: un grupo -(CH₂)ₛ-NR¹⁶R¹⁷ donde s es un entero en el rango entre 1 y 4 y R¹⁶ y R¹⁷ se seleccionan en forma independiente entre hidrógeno o C₁₋₄ alquilo; y un sistema de anillos heterocíclico monocíclico, bicíclico o tricíclico saturado que contiene un heteroátomo N o grupo NR¹⁸ donde R¹⁸ se selecciona entre C₁₋₄ alquilo y bencilo; sus N-óxidos en el anillo piridina; derivados deuterados; y sales farmacéuticamente aceptables, o solvatos del mismo.
ARP140104520A 2013-12-05 2014-12-04 Derivados de heteroarilo AR098621A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
EP13195930 2013-12-05

Publications (1)

Publication Number Publication Date
AR098621A1 true AR098621A1 (es) 2016-06-01

Family

ID=49726580

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP140104520A AR098621A1 (es) 2013-12-05 2014-12-04 Derivados de heteroarilo

Country Status (11)

Country Link
US (1) US9133185B2 (es)
EP (1) EP3077385B1 (es)
KR (1) KR20160086351A (es)
CN (1) CN105793250A (es)
AR (1) AR098621A1 (es)
CA (1) CA2932487A1 (es)
ES (1) ES2655047T3 (es)
HK (1) HK1225385A1 (es)
RU (1) RU2016121854A (es)
TW (1) TW201607944A (es)
WO (1) WO2015082616A1 (es)

Families Citing this family (8)

* 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
WO2016177849A1 (en) 2015-05-07 2016-11-10 Chiesi Farmaceutici S.P.A. Aminoester derivatives
AR104829A1 (es) * 2015-06-01 2017-08-16 Chiesi Farm Spa Derivados de aminoésteres
AR104822A1 (es) 2015-06-01 2017-08-16 Chiesi Farm Spa Derivado de aminoésteres
CN110117271A (zh) * 2018-02-06 2019-08-13 中国科学院上海药物研究所 四氢异喹啉类化合物、其制备方法、包含此类化合物的药物组合物及其用途
WO2020019952A1 (zh) * 2018-07-26 2020-01-30 四川海思科制药有限公司 一种含格隆铵盐及茚达特罗盐的气雾剂药物组合物及其制备方法与应用
KR102191941B1 (ko) 2020-08-19 2020-12-16 이두재 곡물 착유용 자동화 장치

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
RU2617401C2 (ru) * 2011-10-21 2017-04-25 КЬЕЗИ ФАРМАЧЕУТИЧИ С.п.А. Производные 1-фенил 2-пиридинилалкиловых спиртов в качестве ингибиторов фосфодиэстеразы
TW201439089A (zh) 2012-12-05 2014-10-16 Chiesi Farma Spa 新穎化合物
TW201434817A (zh) 2012-12-05 2014-09-16 Chiesi Farma Spa 新穎化合物
BR112015012949A2 (pt) 2012-12-05 2017-07-11 Chiesi Farm Spa composto, composição farmaceutica, uso de um composto, dispositivo inalatório e kit

Also Published As

Publication number Publication date
US20150158858A1 (en) 2015-06-11
ES2655047T3 (es) 2018-02-16
EP3077385B1 (en) 2017-10-04
EP3077385A1 (en) 2016-10-12
RU2016121854A3 (es) 2018-08-23
CN105793250A (zh) 2016-07-20
HK1225385A1 (zh) 2017-09-08
CA2932487A1 (en) 2015-06-11
RU2016121854A (ru) 2017-12-07
WO2015082616A1 (en) 2015-06-11
TW201607944A (zh) 2016-03-01
US9133185B2 (en) 2015-09-15
KR20160086351A (ko) 2016-07-19

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