MX2021000270A - Derivados de la tirosina amida como inhibidores de la rho- cinasa. - Google Patents

Derivados de la tirosina amida como inhibidores de la rho- cinasa.

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Publication number
MX2021000270A
MX2021000270A MX2021000270A MX2021000270A MX2021000270A MX 2021000270 A MX2021000270 A MX 2021000270A MX 2021000270 A MX2021000270 A MX 2021000270A MX 2021000270 A MX2021000270 A MX 2021000270A MX 2021000270 A MX2021000270 A MX 2021000270A
Authority
MX
Mexico
Prior art keywords
compounds
rho
kinase inhibitors
amide derivatives
pulmonary
Prior art date
Application number
MX2021000270A
Other languages
English (en)
Inventor
Fabio Rancati
Anna Maria Capelli
Alessandro Accetta
David Edward Clark
Patrizia Tisselli
Christine Edwards
Gurdip Bhalay
Arnaud Jean Francois Auguste Cheguillaume
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 MX2021000270A publication Critical patent/MX2021000270A/es

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    • 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
    • C07D471/04Ortho-condensed systems
    • 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
    • A61K31/4353Heterocyclic 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 ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/437Heterocyclic 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 ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
    • 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
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445Non condensed piperidines, e.g. piperocaine
    • A61K31/4523Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/4545Non 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
    • 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
    • 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
    • A61K31/519Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/0012Galenical forms characterised by the site of application
    • A61K9/007Pulmonary tract; Aromatherapy
    • A61K9/0073Sprays or powders for inhalation; Aerolised or nebulised preparations generated by other means than thermal energy
    • A61K9/0075Sprays 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/0012Galenical forms characterised by the site of application
    • A61K9/007Pulmonary tract; Aromatherapy
    • A61K9/0073Sprays or powders for inhalation; Aerolised or nebulised preparations generated by other means than thermal energy
    • A61K9/0078Sprays or powders for inhalation; Aerolised or nebulised preparations generated by other means than thermal energy for inhalation via a nebulizer such as a jet nebulizer, ultrasonic nebulizer, e.g. in the form of aqueous drug solutions or dispersions
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/0012Galenical forms characterised by the site of application
    • A61K9/007Pulmonary tract; Aromatherapy
    • A61K9/0073Sprays or powders for inhalation; Aerolised or nebulised preparations generated by other means than thermal energy
    • A61K9/008Sprays or powders for inhalation; Aerolised or nebulised preparations generated by other means than thermal energy comprising drug dissolved or suspended in liquid propellant for inhalation via a pressurized metered dose inhaler [MDI]
    • 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D487/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04Ortho-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D519/00Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00

Abstract

La invención se relaciona con los compuestos de la fórmula que inhibe Rho Cinasa que son derivados bicíclicos de dihidropirimidina-carboxamida, métodos de preparación de tales compuestos, composiciones farmacéuticas que los contienen y su uso terapéutico. En particular, los compuestos de la invención pueden ser útiles en el tratamiento de muchos trastornos asociados a los mecanismos de las enzimas ROCK, como las enfermedades pulmonares, incluido el asma, la enfermedad pulmonar obstructiva crónica (EPOC), la fibrosis pulmonar idiopática (IPF) y la hipertensión arterial pulmonar (PAH).
MX2021000270A 2018-07-16 2019-07-12 Derivados de la tirosina amida como inhibidores de la rho- cinasa. MX2021000270A (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
EP18183733 2018-07-16
PCT/EP2019/068832 WO2020016129A1 (en) 2018-07-16 2019-07-12 Tyrosine amide derivatives as rho- kinase inhibitors

Publications (1)

Publication Number Publication Date
MX2021000270A true MX2021000270A (es) 2021-03-26

Family

ID=62975943

Family Applications (1)

Application Number Title Priority Date Filing Date
MX2021000270A MX2021000270A (es) 2018-07-16 2019-07-12 Derivados de la tirosina amida como inhibidores de la rho- cinasa.

Country Status (13)

Country Link
US (1) US20210284639A1 (es)
EP (1) EP3823969A1 (es)
JP (1) JP2021529819A (es)
KR (1) KR20210032977A (es)
CN (1) CN112752757B (es)
AR (1) AR115766A1 (es)
AU (1) AU2019304472A1 (es)
BR (1) BR112021000101A2 (es)
CA (1) CA3104955A1 (es)
MA (1) MA53164A (es)
MX (1) MX2021000270A (es)
TW (1) TW202019923A (es)
WO (1) WO2020016129A1 (es)

Families Citing this family (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP4263548A1 (en) 2020-12-15 2023-10-25 Chiesi Farmaceutici S.p.A. Dihydrofuropyridine derivatives as rho- kinase inhibitors
CA3202126A1 (en) 2020-12-15 2022-06-23 Fabio Rancati Dihydrofuropyridine derivatives as rho- kinase inhibitors
AU2021402528A1 (en) 2020-12-15 2023-07-27 Chiesi Farmaceutici S.P.A. Dihydrofuropyridine derivatives as rho- kinase inhibitors
WO2023110700A1 (en) 2021-12-13 2023-06-22 Chiesi Farmaceutici S.P.A. Dihydrofuropyridine derivatives as rho-kinase inhibitors

Family Cites Families (13)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US7737153B2 (en) 2002-10-28 2010-06-15 Bayer Schering Pharma Aktiengesellschaft Heteroaryloxy-substituted phenylaminopyrimidines as rho-kinase inhibitors
US7521465B2 (en) * 2003-01-17 2009-04-21 Bexel Pharmaceuticals, Inc. Diphenyl ether derivatives
DE102004017438A1 (de) * 2004-04-08 2005-11-03 Bayer Healthcare Ag Hetaryloxy-substituierte Phenylaminopyrimidine
WO2006009889A1 (en) 2004-06-17 2006-01-26 Smithkline Beecham Corporation Novel inhibitors of rho-kinases
KR20080040027A (ko) * 2005-09-02 2008-05-07 아스테라스 세이야쿠 가부시키가이샤 Rock 억제제로서 아미드 유도체
CA2709918A1 (en) 2007-12-21 2009-06-25 The Scripps Research Institute Benzopyrans and analogs as rho kinase inhibitors
EP2100598A1 (en) * 2008-03-13 2009-09-16 Laboratorios Almirall, S.A. Inhalation composition containing aclidinium for treatment of asthma and chronic obstructive pulmonary disease
EP2331507A2 (en) 2008-09-18 2011-06-15 Astellas Pharma Inc. Heterocyclic carboxamide compounds
ES2622519T3 (es) 2010-07-14 2017-07-06 Novartis Ag Componentes heterocíclicos agonistas del receptor IP
EP2718281B1 (en) * 2011-06-10 2015-09-09 Chiesi Farmaceutici S.p.A. Compounds having muscarinic receptor antagonist and beta2 adrenergic receptor agonist activity
US9682963B2 (en) 2013-01-29 2017-06-20 Redx Pharma Plc Pyridine derivatives as soft rock inhibitors
AR110401A1 (es) 2016-12-21 2019-03-27 Chiesi Farm Spa Derivados dihidropirimidina bicíclica-carboxamida como inhibidores de rho-quinasa
WO2018138293A1 (en) * 2017-01-30 2018-08-02 Chiesi Farmaceutici S.P.A. Tyrosine amide derivatives as rho- kinase inhibitors

Also Published As

Publication number Publication date
AU2019304472A1 (en) 2021-02-11
US20210284639A1 (en) 2021-09-16
JP2021529819A (ja) 2021-11-04
BR112021000101A2 (pt) 2021-03-30
CA3104955A1 (en) 2020-01-23
EP3823969A1 (en) 2021-05-26
CN112752757A (zh) 2021-05-04
AR115766A1 (es) 2021-02-24
WO2020016129A1 (en) 2020-01-23
TW202019923A (zh) 2020-06-01
CN112752757B (zh) 2024-01-12
MA53164A (fr) 2021-05-26
KR20210032977A (ko) 2021-03-25

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