Search International and National Patent Collections
Some content of this application is unavailable at the moment.
If this situation persists, please contact us atFeedback&Contact
1. (AR103990) UREAS CÍCLICAS COMO INHIBIDORAS DE ROCK

Office : Argentina
Application Number: P160100053 Application Date: 08.01.2016
Publication Number: 103990 Publication Date: 21.06.2017
Publication Kind : A1
IPC:
C07D 403/10
C07D 403/14
C07D 401/10
C07D 401/14
C07D 471/04
C07D 487/04
C07D 405/10
C07D 405/14
C07D 413/10
C07D 413/14
A61K 31/4178
A61K 31/422
A61P 9/00
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
403
Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/167
02
containing two hetero rings
10
linked by a carbon chain containing aromatic rings
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
403
Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/167
14
containing three or more hetero rings
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
401
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
02
containing two hetero rings
10
linked by a carbon chain containing aromatic rings
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
401
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
14
containing three or more hetero rings
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
471
Heterocyclic 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/-C07D463/251
02
in which the condensed system contains two hetero rings
04
Ortho-condensed systems
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
487
Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/-C07D477/183
02
in which the condensed system contains two hetero rings
04
Ortho-condensed systems
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
405
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
02
containing two hetero rings
10
linked by a carbon chain containing aromatic rings
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
405
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
14
containing three or more hetero rings
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
413
Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
02
containing two hetero rings
10
linked by a carbon chain containing aromatic rings
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
413
Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
14
containing three or more hetero rings
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
K
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31
Medicinal preparations containing organic active ingredients
33
Heterocyclic compounds
395
having nitrogen as a ring hetero atom, e.g. guanethidine, rifamycins
41
having five-membered rings with two or more ring hetero atoms, at least one of which is nitrogen, e.g. tetrazole
4164
1,3-Diazoles
4178
not condensed and containing further heterocyclic rings, e.g. pilocarpine, nitrofurantoin
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
K
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31
Medicinal preparations containing organic active ingredients
33
Heterocyclic compounds
395
having nitrogen as a ring hetero atom, e.g. guanethidine, rifamycins
41
having five-membered rings with two or more ring hetero atoms, at least one of which is nitrogen, e.g. tetrazole
42
Oxazoles
422
not condensed and containing further heterocyclic rings
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
P
SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
9
Drugs for disorders of the cardiovascular system
Applicants: BRISTOL-MYERS SQUIBB COMPANY
Inventors: RAJEEV S. BHIDE
PRASANNA SAVANOR MADDU RAO
KUMARESAN CHINNAKOTTI SANKARANKOVIL
SHARANABASAPPA PATIL
NAVNATH DNYANOBA YADAV
MANDAR SHRIKRISHNA BODAS
PETER W. GLUNZ
DOREE F. SITKOFF
JEEVANPRAKASH SHETTY

Priority Data: 62/101434 09.01.2015 US
Title: (ES) UREAS CÍCLICAS COMO INHIBIDORAS DE ROCK
Abstract:
(ES) Estos compuestos son inhibidores de ROCK selectivos. También se refiere a composiciones farmacéuticas que comprenden estos compuestos y a métodos para tratar trastornos cardiovasculares, trastornos relacionados con el músculo liso, trastornos oncológicos, trastornos neuropatológicos, trastornos autoinmunitarios, trastornos fibróticos y/o trastornos inflamatorios mediante su uso. Reivindicación 1: Un compuesto caracterizado porque tiene la fórmula (1) o un enantiómero, diastereómero, estereoisómero, tautómero, sal de aquel aceptable desde el punto de vista farmacéutico, en donde - - - es un enlace opcional; el anillo A se selecciona independientemente de los compuestos del grupo de fórmulas (2); J¹, J², J³ y J⁴ se seleccionan independientemente de N y CR³, siempre que no más de dos de J¹, J², J³ y J⁴ sean N; K se selecciona independientemente de N y CR¹; R¹ se selecciona independientemente de H, F, Cl, Br, OH, CN, NRᵃRᵃ, -OC₁₋₄ alquilo sustituido con 0 - 3 Rᵉ y C₁₋₄ alquilo sustituido con 0 - 3 Rᵉ; R² se selecciona independientemente de H, (CH₂)ʳORᵇ, (CH₂)ʳS(O)ₚRᶜ, (CH₂)ʳC(=O)Rᵇ, (CH₂)ʳNRᵃRᵃ, (CH₂)ʳCN, (CH₂)ʳC(=O)NRᵃRᵃ, (CH₂)ʳNRᵃC(=O)Rᵇ, (CH₂)ʳNRᵃC(=O)NRᵃRᵃ, (CH₂)ʳNRᵃC(=O)ORᵇ, (CH₂)ʳOC(=O)NRᵃRᵃ, (CH₂)ʳC(=O)ORᵇ, (CH₂)ʳS(O)ₚNRᵃRᵃ, (CH₂)ʳNRᵃS(O)ₚNRᵃRᵃ, (CH₂)ʳNRᵃS(O)ₚRᶜ, (CH₂)ʳC₃₋₆ carbociclilo sustituido con 0 - 3 Rᵉ y (CH₂)ʳheterociclilo sustituido con 0 - 3 Rᵉ; R³ se selecciona independientemente de H, F, Cl, Br, CN, C₁₋₄ alquilo sustituido con 0 - 3 Rᵉ, (CH₂)ʳORᵇ, (CH₂)ʳS(O)ₚRᶜ, (CH₂)ʳC(=O)Rᵇ, (CH₂)ʳNRᵃRᵃ, (CH₂)ʳC(=O)NRᵃRᵃ, (CH₂)ʳC(=O)(CH₂)ʳNRᵃRᵃ, (CH₂)ʳCN, (CH₂)ʳNRᵃC(=O)Rᵇ, (CH₂)ʳNRᵃC(=O)ORᵇ, (CH₂)ʳOC(=O)NRᵃRᵃ, (CH₂)ʳNRᵃC(=O)NRᵃRᵃ, (CH₂)ʳC(=O)ORᵇ, (CH₂)ʳS(O)ₚNRᵃRᵃ, (CH₂)ʳNRᵃS(O)ₚNRᵃRᵃ, (CH₂)ʳNRᵃS(O)ₚRᶜ, (CH₂)ʳC₃₋₆ carbociclilo sustituido con 0 - 3 Rᵉ y (CH₂)ʳheterociclilo sustituido con 0 - 3 Rᵉ; R⁴ se selecciona independientemente de H, F, Cl, Br, OH, CN, OC₁₋₄ alquilo sustituido con 0 - 3 Rᵉ, NRᵃRᵃ y C₁₋₄ alquilo sustituido con 0 - 3 Rᵉ; R⁵ se selecciona independientemente de H, =O, C₁₋₄ alquilo sustituido con 0 - 4 Rᵉ, (CH₂)ʳORᵇ, (CH₂)ʳS(O)ₚRᶜ, (CH₂)ʳC(=O)Rᵇ, (CH₂)ʳNRᵃRᵃ, (CH₂)ʳCN, (CH₂)ʳC(=O)NRᵃRᵃ, (CH₂)ʳNRᵃC(=O)Rᵇ, (CH₂)ʳNRᵃC(=O)NRᵃRᵃ, (CH₂)ʳNRᵃC(=O)ORᵇ, (CH₂)ʳOC(=O)NRᵃRᵃ, (CH₂)ʳC(=O)ORᵇ, (CH₂)ʳS(O)ₚNRᵃRᵃ, (CH₂)ʳNRᵃS(O)ₚNRᵃRᵃ, (CH₂)ʳNRᵃS(O)ₚRᶜ, (CH₂)ʳC₃₋₆ carbociclilo sustituido con 0 - 3 Rᵉ y (CH₂)ʳheterociclilo sustituido con 0 - 3 Rᵉ; R⁶ y R⁷ se seleccionan independientemente de H, C₁₋₄ alquilo sustituido con 0 - 4 Rᵉ, (CH₂)ʳORᵇ, (CH₂)ʳS(O)ₚRᶜ, (CH₂)ʳC(=O)Rᵇ, (CH₂)ʳNRᵃRᵃ, (CH₂)ʳC(=O)NRᵃRᵃ, (CH₂)ʳC(O)(CH₂)ʳNRᵃRᵃ, (CH₂)ʳNRᵃC(=O)Rᵇ, (CH₂)ʳNRᵃC(=O)ORᵇ, (CH₂)ʳOC(=O)NRᵃRᵃ, (CH₂)ʳNRᵃC(=O)NRᵃRᵃ, (CH₂)ʳC(=O)ORᵇ, (CH₂)ʳS(O)ₚNRᵃRᵃ, (CH₂)ʳNRᵃS(O)ₚRᶜ, (CH₂)ʳC₃₋₆ carbociclilo sustituido con 0 - 3 Rᵉ y (CH₂)ʳheterociclilo sustituido con 0 - 3 Rᵉ; R⁸ se selecciona independientemente de C₃₋₆ cicloalquilo, heterociclilo, arilo y heteroarilo cada uno sustituido con 0 - 5 R⁹; R⁹ se selecciona independientemente de F, Cl, Br, C₁₋₄ alquilo, C₂₋₄ alquenilo, C₂₋₄ alquinilo, nitro, -(CHRᵈ)ʳS(O)ₚRᶜ, -(CHRᵈ)ʳS(O)ₚNRᵃRᵃ, -(CHRᵈ)ʳNRᵃS(O)ₚRᶜ, -(CHRᵈ)ʳORᵇ, -(CHRᵈ)ʳCN, -(CHRᵈ)ʳNRᵃRᵃ, -(CHRᵈ)ʳNRᵃC(=O)Rᵇ, -(CHRᵈ)ʳNRᵃC(=O)NRᵃRᵃ, -(CHRᵈ)ʳC(=O)ORᵇ, -(CHRᵈ)ʳC(=O)Rᵇ, -(CHRᵈ)ʳOC(=O)Rᵇ, -(CHRᵈ)ʳ-cicloalquilo, -(CHRᵈ)ʳ-heterociclilo, -(CHRᵈ)ʳ-arilo y -(CHRᵈ)ʳ-heteroarilo, en donde el alquilo, cicloalquilo, heterociclilo, arilo o heteroarilo se sustituye con 0 - 4 Rᵉ; Rᵃ, en cada caso, se selecciona independientemente de H, C₁₋₆ alquilo sustituido con 0 - 5 Rᵉ, C₂₋₆ alquenilo sustituido con 0 - 5 Rᵉ, C₂₋₆ alquinilo sustituido con 0 - 5 Rᵉ, (CH₂)ʳC₃₋₁₀ carbociclilo sustituido con 0 - 5 Rᵉ y (CH₂)ʳheterociclilo sustituido con 0 - 5 Rᵉ; o Rᵃ y Rᵃ, junto con el átomo de nitrógeno al que están unidos, forman un anillo heterocíclico sustituido con 0 - 5 Rᵉ; Rᵇ, en cada caso, se selecciona independientemente de H, C₁₋₆ alquilo sustituido con 0 - 5 Rᵉ, C₂₋₆ alquenilo sustituido con 0 - 5 Rᵉ, C₂₋₆ alquinilo sustituido con 0 - 5 Rᵉ, (CH₂)ʳC₃₋₁₀ carbociclilo sustituido con 0 - 5 Rᵉ y (CH₂)ʳheterociclilo sustituido con 0 - 5 Rᵉ; Rᶜ, en cada caso, se selecciona independientemente de C₁₋₆ alquilo sustituido con 0 - 5 Rᵉ, C₂₋₆ alquenilo sustituido con 0 - 5 Rᵉ, C₂₋₆ alquinilo sustituido con 0 - 5 Rᵉ, C₃₋₆ carbociclilo y heterociclilo; Rᵈ, en cada caso, se selecciona independientemente de H y C₁₋₄ alquilo sustituido con 0 - 5 Rᵉ; Rᵉ, en cada caso, se selecciona independientemente de C₁₋₆ alquilo sustituido con 0 - 5 Rᶠ, C₂₋₆ alquenilo, C₂₋₆ alquinilo, (CH₂)ʳC₃₋₆ cicloalquilo, (CH₂)ʳC₄₋₆ heterociclilo, (CH₂)ʳarilo, (CH₂)ʳheteroarilo, F, Cl, Br, CN, NO₂, =O, CO₂H, (CH₂)ʳORᶠ, S(O)ₚRᶠ, C(=O)NRᶠRᶠ, NRᶠC(=O)Rᵈ, S(O)ₚNRᶠRᶠ, NRᶠS(O)ₚRᵈ, NRᶠC(=O)ORᵈ, OC(=O)NRᶠRᶠ y (CH₂)ʳNRᶠRᶠ; Rᶠ, en cada caso, se selecciona independientemente de H, F, Cl, Br, CN, OH, C₁₋₅ alquilo, C₃₋₆ cicloalquilo y fenilo, o Rᶠ y Rᶠ, junto con el átomo de nitrógeno al que están unidos, forman un anillo heterocíclico opcionalmente sustituido con C₁₋₄ alquilo; n se selecciona independientemente de 1, 2 y 3; p, en cada caso, se selecciona independientemente de 0, 1 y 2; r, en cada caso, se selecciona independientemente de 0, 1, 2, 3 y 4; y siempre que (i) R⁹ no sea una piperazina sustituida; (ii) cuando n sea 3, R⁸ no sea un resto de fórmula (3); y (iii) cuando A sea el compuesto de fórmula (4), R² no sea C(=O)NRᵃRᵃ, NRᵃC(O)Rᵇ y -NRᵃC(=O)NRᵃRᵃ.
Also published as:
CN107406426US20180000788JP2018501285IN201717028119WO/2016/112236