AR103990A1 - Ureas cíclicas como inhibidoras de rock - Google Patents
Ureas cíclicas como inhibidoras de rockInfo
- Publication number
- AR103990A1 AR103990A1 ARP160100053A ARP160100053A AR103990A1 AR 103990 A1 AR103990 A1 AR 103990A1 AR P160100053 A ARP160100053 A AR P160100053A AR P160100053 A ARP160100053 A AR P160100053A AR 103990 A1 AR103990 A1 AR 103990A1
- Authority
- AR
- Argentina
- Prior art keywords
- substituted
- independently selected
- nrara
- chrd
- rnrac
- Prior art date
Links
- 239000003112 inhibitor Substances 0.000 title abstract 2
- 150000003672 ureas Chemical class 0.000 title 1
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 abstract 8
- 125000004452 carbocyclyl group Chemical group 0.000 abstract 6
- 125000000623 heterocyclic group Chemical group 0.000 abstract 6
- 101150105130 RORB gene Proteins 0.000 abstract 5
- 150000001875 compounds Chemical class 0.000 abstract 5
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 abstract 4
- 125000000882 C2-C6 alkenyl group Chemical group 0.000 abstract 4
- 125000003601 C2-C6 alkynyl group Chemical group 0.000 abstract 4
- 125000000217 alkyl group Chemical group 0.000 abstract 4
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 abstract 4
- 208000035475 disorder Diseases 0.000 abstract 4
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 abstract 2
- 125000003118 aryl group Chemical group 0.000 abstract 2
- 125000000753 cycloalkyl group Chemical group 0.000 abstract 2
- 125000001072 heteroaryl group Chemical group 0.000 abstract 2
- 229910052757 nitrogen Inorganic materials 0.000 abstract 2
- 125000004433 nitrogen atom Chemical group N* 0.000 abstract 2
- 125000006656 (C2-C4) alkenyl group Chemical group 0.000 abstract 1
- 125000006650 (C2-C4) alkynyl group Chemical group 0.000 abstract 1
- 125000006706 (C3-C6) carbocyclyl group Chemical group 0.000 abstract 1
- 208000023275 Autoimmune disease Diseases 0.000 abstract 1
- 208000024172 Cardiovascular disease Diseases 0.000 abstract 1
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 abstract 1
- GLUUGHFHXGJENI-UHFFFAOYSA-N diethylenediamine Natural products C1CNCCN1 GLUUGHFHXGJENI-UHFFFAOYSA-N 0.000 abstract 1
- 230000003176 fibrotic effect Effects 0.000 abstract 1
- 208000027866 inflammatory disease Diseases 0.000 abstract 1
- 230000002981 neuropathic effect Effects 0.000 abstract 1
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 abstract 1
- 230000000771 oncological effect Effects 0.000 abstract 1
- 239000008194 pharmaceutical composition Substances 0.000 abstract 1
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 abstract 1
- 150000004885 piperazines Chemical class 0.000 abstract 1
- 239000011435 rock Substances 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 210000002460 smooth muscle Anatomy 0.000 abstract 1
Classifications
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- 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
- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
- A61K31/4164—1,3-Diazoles
- A61K31/4178—1,3-Diazoles not condensed 1,3-diazoles and containing further heterocyclic rings, e.g. pilocarpine, nitrofurantoin
-
- 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
- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
- A61K31/42—Oxazoles
- A61K31/422—Oxazoles not condensed and containing further heterocyclic rings
-
- 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
- A61K31/498—Pyrazines or piperazines ortho- and peri-condensed with carbocyclic ring systems, e.g. quinoxaline, phenazine
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P37/00—Drugs for immunological or allergic disorders
- A61P37/02—Immunomodulators
- A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/04—Inotropic agents, i.e. stimulants of cardiac contraction; Drugs for heart failure
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/12—Antihypertensives
-
- 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
- C07D401/10—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 carbon chain containing aromatic rings
-
- 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
- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
- C07D403/10—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a carbon chain containing aromatic 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
- C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
- C07D413/10—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a carbon chain containing aromatic rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D471/00—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 C07D451/00 - C07D463/00
- C07D471/02—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 C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
- C07D471/04—Ortho-condensed systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
- C07D487/02—Heterocyclic 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
- C07D487/04—Ortho-condensed systems
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- General 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)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Epidemiology (AREA)
- Cardiology (AREA)
- Heart & Thoracic Surgery (AREA)
- Immunology (AREA)
- Transplantation (AREA)
- Hospice & Palliative Care (AREA)
- Vascular Medicine (AREA)
- Pain & Pain Management (AREA)
- Rheumatology (AREA)
- Urology & Nephrology (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Plural Heterocyclic Compounds (AREA)
Abstract
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.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201562101434P | 2015-01-09 | 2015-01-09 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR103990A1 true AR103990A1 (es) | 2017-06-21 |
Family
ID=55310909
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP160100053A AR103990A1 (es) | 2015-01-09 | 2016-01-08 | Ureas cíclicas como inhibidoras de rock |
Country Status (8)
| Country | Link |
|---|---|
| US (1) | US10123993B2 (es) |
| EP (1) | EP3242873B1 (es) |
| JP (1) | JP6779214B2 (es) |
| CN (1) | CN107406426B (es) |
| AR (1) | AR103990A1 (es) |
| ES (1) | ES2815681T3 (es) |
| TW (1) | TW201630899A (es) |
| WO (1) | WO2016112236A1 (es) |
Families Citing this family (27)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN107406426B (zh) | 2015-01-09 | 2020-11-20 | 百时美施贵宝公司 | 作为rock抑制剂的环状脲类 |
| EP3268360B1 (en) * | 2015-03-09 | 2019-04-24 | Bristol-Myers Squibb Company | Lactams as inhibitors of rock |
| WO2017046739A1 (en) * | 2015-09-15 | 2017-03-23 | Glaxosmithkline Intellectual Property (No.2) Limited | Imidazolidinone derivatives as inhibitors of perk |
| UY37073A (es) | 2016-01-13 | 2017-07-31 | Bristol-Myers Squibb Company Una Corporación Del Estado De Delaware | Salicilamidas espiroheptanos y compuestos relacionados como inhibidores de rock, y las composiciones que los contienen |
| US10562887B2 (en) | 2016-05-27 | 2020-02-18 | Bristol-Myers Squibb Company | Triazolones and tetrazolones as inhibitors of ROCK |
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- 2016-01-08 JP JP2017536259A patent/JP6779214B2/ja active Active
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| JP2018501285A (ja) | 2018-01-18 |
| ES2815681T3 (es) | 2021-03-30 |
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| CN107406426B (zh) | 2020-11-20 |
| CN107406426A (zh) | 2017-11-28 |
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| EP3242873B1 (en) | 2020-07-22 |
| JP6779214B2 (ja) | 2020-11-04 |
| EP3242873A1 (en) | 2017-11-15 |
| TW201630899A (zh) | 2016-09-01 |
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