PE20191744A1 - Derivados de tirosinamida como inhibidores de rho-quinasa - Google Patents

Derivados de tirosinamida como inhibidores de rho-quinasa

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Publication number
PE20191744A1
PE20191744A1 PE2019001481A PE2019001481A PE20191744A1 PE 20191744 A1 PE20191744 A1 PE 20191744A1 PE 2019001481 A PE2019001481 A PE 2019001481A PE 2019001481 A PE2019001481 A PE 2019001481A PE 20191744 A1 PE20191744 A1 PE 20191744A1
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PE
Peru
Prior art keywords
haloalkyl
independently
tyrosinamide
compounds
halogen
Prior art date
Application number
PE2019001481A
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English (en)
Inventor
Alessandro Accetta
Fabio Rancati
Anna Maria Capelli
David Edward Clark
Patrizia Tisselli
Christine Edwards
Arnaud Jean Francois Auguste Cheguillaume
Gurdip Bhalay
Original Assignee
Chiesi Farm Spa
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Publication date
Application filed by Chiesi Farm Spa filed Critical Chiesi Farm Spa
Publication of PE20191744A1 publication Critical patent/PE20191744A1/es

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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
    • A61K31/4353Heterocyclic 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
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    • 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
    • A61K31/4375Heterocyclic 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 six-membered ring having nitrogen as a ring heteroatom, e.g. quinolizines, naphthyridines, berberine, vincamine
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    • A61K31/439Heterocyclic 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 the ring forming part of a bridged ring system, e.g. quinuclidine
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    • 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
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    • 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
    • A61K31/47Quinolines; Isoquinolines
    • A61K31/472Non-condensed isoquinolines, e.g. papaverine
    • A61K31/4725Non-condensed isoquinolines, e.g. papaverine containing further heterocyclic rings
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    • A61K31/496Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
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    • A61K31/498Pyrazines or piperazines ortho- and peri-condensed with carbocyclic ring systems, e.g. quinoxaline, phenazine
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    • A61K31/4985Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring systems
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    • A61K31/50Pyridazines; Hydrogenated pyridazines
    • A61K31/501Pyridazines; Hydrogenated pyridazines not condensed and containing further heterocyclic rings
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    • 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
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    • A61K31/535Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/53751,4-Oxazines, e.g. morpholine
    • A61K31/53771,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
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    • A61K31/53751,4-Oxazines, e.g. morpholine
    • A61K31/53831,4-Oxazines, e.g. morpholine ortho- or peri-condensed with heterocyclic ring systems
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  • Heart & Thoracic Surgery (AREA)
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  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
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Abstract

Referido a un compuesto de formula I, en donde X1 y X2 son independientemente un grupo CH o N; p es 0, 1, 2 o 3; cada R cuando esta presente es halogeno; R0 y R1 es independientemente -H, halogeno, -CN, entre otros; R2 y R3 son iguales o diferentes, son -H, (C1-C6)alquilo, (C1-C6)haloalquilo, entre otros; R4 y R5 son independientemente H, (C1-C6)haloalquilo; (C1-C6)alcoxi, entre otros; R6 es -H, (C1-C6)alquilo, (C1-C6)haloalquilo; o sus sales aceptables farmaceuticamente y solvatos. Un compuesto preferido es (S)-2-amino-3-(3-fluoro-4-((3-metil-1H-pirrolo[2,3-b]piridin-4-il)oxi)fenil)-N-(1-metilpiperidin-4-il)propanamida. Estos compuestos derivados de tirosinamida inhiben la rho-quinasa. Tambien se refiere a metodos para preparar dichos compuestos, una composicion farmaceutica que comprende dichos compuestos, ya sea solo o en combinacion con otro ingrediente activo y su uso en el tratamiento de numerosos trastornos asociados con mecanismos relacionados con las enzimas ROCK, como por ejemplo enfermedades pulmonares que incluyen asma, enfermedad pulmonar obstructiva cronica (EPOC), entre otros.
PE2019001481A 2017-01-30 2018-01-26 Derivados de tirosinamida como inhibidores de rho-quinasa PE20191744A1 (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
EP17153785 2017-01-30
PCT/EP2018/052009 WO2018138293A1 (en) 2017-01-30 2018-01-26 Tyrosine amide derivatives as rho- kinase inhibitors

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PE20191744A1 true PE20191744A1 (es) 2019-12-12

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US (2) US10501461B2 (es)
EP (1) EP3573987B1 (es)
JP (1) JP7208142B2 (es)
KR (1) KR102429419B1 (es)
CN (1) CN110248939B (es)
AR (1) AR110782A1 (es)
AU (1) AU2018212593B2 (es)
BR (1) BR112019015707A2 (es)
CA (1) CA3047212A1 (es)
CL (1) CL2019002103A1 (es)
CO (1) CO2019008986A2 (es)
EA (1) EA039783B1 (es)
ES (1) ES2866152T3 (es)
IL (1) IL268004B (es)
MX (1) MX2019008895A (es)
MY (1) MY195588A (es)
PE (1) PE20191744A1 (es)
PH (1) PH12019501572A1 (es)
PL (1) PL3573987T3 (es)
SA (1) SA519402319B1 (es)
SG (1) SG11201906134YA (es)
TW (1) TW201831481A (es)
WO (1) WO2018138293A1 (es)
ZA (1) ZA201904239B (es)

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IL268004A (en) 2019-09-26
ZA201904239B (en) 2020-12-23
CN110248939B (zh) 2022-05-17
JP7208142B2 (ja) 2023-01-18
SG11201906134YA (en) 2019-08-27
EP3573987B1 (en) 2021-03-10
TW201831481A (zh) 2018-09-01
ES2866152T3 (es) 2021-10-19
CO2019008986A2 (es) 2020-01-17
US20180215758A1 (en) 2018-08-02
KR102429419B1 (ko) 2022-08-05
WO2018138293A1 (en) 2018-08-02
PH12019501572A1 (en) 2020-03-16
US10954236B2 (en) 2021-03-23
CN110248939A (zh) 2019-09-17
EA201991793A1 (ru) 2020-03-20
SA519402319B1 (ar) 2022-03-02
CA3047212A1 (en) 2018-08-02
EP3573987A1 (en) 2019-12-04
US20200079774A1 (en) 2020-03-12
EA039783B1 (ru) 2022-03-14
MY195588A (en) 2023-02-02
CL2019002103A1 (es) 2019-12-27

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