AR114926A1 - Derivados de azaindol como inhibidores de rho-quinasa - Google Patents
Derivados de azaindol como inhibidores de rho-quinasaInfo
- Publication number
- AR114926A1 AR114926A1 ARP190101592A ARP190101592A AR114926A1 AR 114926 A1 AR114926 A1 AR 114926A1 AR P190101592 A ARP190101592 A AR P190101592A AR P190101592 A ARP190101592 A AR P190101592A AR 114926 A1 AR114926 A1 AR 114926A1
- Authority
- AR
- Argentina
- Prior art keywords
- alkyl
- group
- integer
- independently
- hydroxyalkyl
- Prior art date
Links
- 239000003590 rho kinase inhibitor Substances 0.000 title 1
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 abstract 9
- 125000006552 (C3-C8) cycloalkyl group Chemical group 0.000 abstract 3
- -1 -OH Chemical group 0.000 abstract 3
- 125000006577 C1-C6 hydroxyalkyl group Chemical group 0.000 abstract 3
- 125000000623 heterocyclic group Chemical group 0.000 abstract 3
- 125000000027 (C1-C10) alkoxy group Chemical group 0.000 abstract 2
- 125000000171 (C1-C6) haloalkyl group Chemical group 0.000 abstract 2
- 125000000217 alkyl group Chemical group 0.000 abstract 2
- 125000003118 aryl group Chemical group 0.000 abstract 2
- 125000005843 halogen group Chemical group 0.000 abstract 2
- 125000001072 heteroaryl group Chemical group 0.000 abstract 2
- 125000001424 substituent group Chemical group 0.000 abstract 2
- 125000000008 (C1-C10) alkyl group Chemical group 0.000 abstract 1
- 125000000882 C2-C6 alkenyl group Chemical group 0.000 abstract 1
- 125000003601 C2-C6 alkynyl group Chemical group 0.000 abstract 1
- 125000003710 aryl alkyl group Chemical group 0.000 abstract 1
- 125000000732 arylene group Chemical group 0.000 abstract 1
- 229910052799 carbon Inorganic materials 0.000 abstract 1
- 125000004432 carbon atom Chemical group C* 0.000 abstract 1
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 abstract 1
- 150000001875 compounds Chemical class 0.000 abstract 1
- 125000006254 cycloalkyl carbonyl group Chemical group 0.000 abstract 1
- 229910052736 halogen Inorganic materials 0.000 abstract 1
- 150000002367 halogens Chemical class 0.000 abstract 1
- 125000005549 heteroarylene group Chemical group 0.000 abstract 1
- 125000000592 heterocycloalkyl group Chemical group 0.000 abstract 1
- 125000002887 hydroxy group Chemical group [H]O* 0.000 abstract 1
- 125000002768 hydroxyalkyl group Chemical group 0.000 abstract 1
- 229910052757 nitrogen Inorganic materials 0.000 abstract 1
- 125000004433 nitrogen atom Chemical group N* 0.000 abstract 1
- 229910052760 oxygen Inorganic materials 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 239000012453 solvate Substances 0.000 abstract 1
- 229910052717 sulfur Inorganic materials 0.000 abstract 1
Classifications
-
- 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
-
- 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
- A61K31/47—Quinolines; Isoquinolines
- A61K31/472—Non-condensed isoquinolines, e.g. papaverine
- A61K31/4725—Non-condensed isoquinolines, e.g. papaverine 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
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim 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
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with 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
- A61K31/535—Heterocyclic 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
- A61K31/5355—Non-condensed oxazines and containing further heterocyclic rings
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K33/00—Medicinal preparations containing inorganic active ingredients
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
- A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/0012—Galenical forms characterised by the site of application
- A61K9/007—Pulmonary tract; Aromatherapy
- A61K9/0073—Sprays or powders for inhalation; Aerolised or nebulised preparations generated by other means than thermal energy
- A61K9/0075—Sprays 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/0012—Galenical forms characterised by the site of application
- A61K9/007—Pulmonary tract; Aromatherapy
- A61K9/0073—Sprays or powders for inhalation; Aerolised or nebulised preparations generated by other means than thermal energy
- A61K9/0078—Sprays 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
-
- 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
- A61P11/06—Antiasthmatics
-
- 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D519/00—Heterocyclic 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
-
- 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
- A61M11/00—Sprayers or atomisers specially adapted for therapeutic purposes
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- General Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Epidemiology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Pulmonology (AREA)
- Otolaryngology (AREA)
- Inorganic Chemistry (AREA)
- Dispersion Chemistry (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
Abstract
Reivindicación 1: Compuestos caracterizados porque son de fórmula (1) en donde X¹ y X² son, cada vez que aparecen, en forma independiente, un grupo CH o un átomo de nitrógeno, p es cero o un número entero de 1 a 3; cada R es independientemente H o halógeno; R¹ es un grupo de fórmula (2), en donde r es 0 o un número entero de 1 a 4; q es 0 o un número entero de 1 a 4; W¹ es un grupo divalente arileno o heteroarileno seleccionado entre A1 - A11 del grupo de fórmulas (3), en donde [1] es el punto de unión de W¹ al resto de la molécula y [2] es el punto de unión a -(CH₂)ʳ-; P está ausente o es un grupo divalente seleccionado entre O, S, SO, SO₂, CO, NR⁶, N(R⁶)(CH₂)ₙSO₂, N(R⁶)COO, N(R⁶)(CH₂)ₙC(O), N(R⁶)(CH₂)ₙO, SO₂N(R⁶), OC(O)N(R⁶) y C(O)N(R⁶), N(R⁶)C(O)N(R⁶); W² es H o se selecciona entre alquilo C₁₋₆, cicloalquilo C₃₋₈, heterocicloalquilo C₃₋₈, arilo, arilalquilo C₁₋₆ y heteroarilo; opcionalmente sustituido por uno o más sustituyentes independientemente seleccionados entre átomos de halógeno, -OH, oxo (=O), -SH, -NO₂, -CN, -CON(R⁶)₂, -C(O)R⁶, -NR⁶C(O)CH₃, -NH₂, -NHCOR⁶, -CO₂R⁶, -SO₂N(R⁶)₂, -NR⁶SO₂CH₃, alquilo C₁₋₆, haloalquilo C₁₋₆, alcoxi C₁₋₁₀, cicloalquilo C₃₋₈ y cicloalquilo C₃₋₆-carbonilo; n es, cada vez que aparece, en forma independiente, 0 o un número entero de 1 a 3; R⁶ es, cada vez que aparece, en forma independiente, H o se selecciona entre alquilo C₁₋₆, haloalquilo C₁₋₆, alquinilo C₂₋₆, alquenilo C₂₋₆, cicloalquilo C₃₋₈, heteroarilo y arilo opcionalmente sustituidos por uno o más sustituyentes seleccionados entre átomos de halógeno, -OH, oxo (=O), -SH, -NO₂, -CN, -CONH₂, -COOH, alquilo C₁₋₁₀ y alcoxi C₁₋₁₀; B es un grupo de fórmula R²R³N-alquilo C₁₋₆, opcionalmente sustituido por uno o más grupos seleccionados entre hidroxilo, alquilo C₁₋₆ e hidroxialquilo C₁₋₆; en donde R² y R³, iguales o diferentes, son H o se seleccionan entre alquilo C₁₋₆, hidroxialquilo C₁₋₆, o B es un grupo de fórmula R⁴R³N-alquilo C₁₋₆, en donde R³ es H, o se selecciona entre alquilo C₁₋₆, hidroxialquilo C₁₋₆ y R⁴ es un grupo alquilo divalente -(CH₂)ₛ-, en donde s es un número entero de 1 a 3, donde dicho grupo alquilo divalente está conectado al átomo de carbono en posición orto en el anillo adyacente para formar un anillo heterocíclico, preferentemente, un anillo heterocíclico de 4 a 10 miembros, fusionado con el anillo adyacente, en donde dicho anillo heterocíclico a su vez está opcionalmente sustituido con uno o más grupos seleccionados entre alquilo C₁₋₆, hidroxialquilo C₁₋₆; y sales y solvatos farmacéuticamente aceptables de los mismos.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP18177556 | 2018-06-13 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR114926A1 true AR114926A1 (es) | 2020-10-28 |
Family
ID=62631021
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP190101592A AR114926A1 (es) | 2018-06-13 | 2019-06-10 | Derivados de azaindol como inhibidores de rho-quinasa |
Country Status (5)
| Country | Link |
|---|---|
| US (1) | US20210253568A1 (es) |
| EP (1) | EP3807273B1 (es) |
| AR (1) | AR114926A1 (es) |
| MA (1) | MA52891A (es) |
| WO (1) | WO2019238628A1 (es) |
Families Citing this family (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| ES3041795T3 (en) | 2020-12-15 | 2025-11-14 | Chiesi Farm Spa | Dihydrofuropyridine derivatives as rho- kinase inhibitors |
| EP4263547B1 (en) | 2020-12-15 | 2025-07-02 | Chiesi Farmaceutici S.p.A. | Dihydrofuropyridine derivatives as rho- kinase inhibitors |
| JP2023552901A (ja) | 2020-12-15 | 2023-12-19 | キエシ・フアルマチエウテイチ・ソチエタ・ペル・アチオニ | Ｒｈｏキナーゼ阻害剤としてのジヒドロフロピリジン誘導体 |
| WO2023110700A1 (en) | 2021-12-13 | 2023-06-22 | Chiesi Farmaceutici S.P.A. | Dihydrofuropyridine derivatives as rho-kinase inhibitors |
Family Cites Families (9)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US5795977A (en) * | 1989-09-15 | 1998-08-18 | Metabasis Therapeutics, Inc. | Water soluble adenosine kinase inhibitors |
| WO2004039796A1 (de) | 2002-10-28 | 2004-05-13 | Bayer Healthcare Ag | Heteroaryloxy-substituierte phenylaminopyrimidine als rho-kinaseinhibitoren |
| DE102004017438A1 (de) | 2004-04-08 | 2005-11-03 | Bayer Healthcare Ag | Hetaryloxy-substituierte Phenylaminopyrimidine |
| JP2008503492A (ja) | 2004-06-17 | 2008-02-07 | スミスクライン・ビーチャム・コーポレイション | Ｒｈｏ−キナーゼの新規阻害剤 |
| US20110150833A1 (en) | 2007-12-21 | 2011-06-23 | The Scripps Research Institute | Benzopyrans and analogs as rho kinase inhibitors |
| MX2011002825A (es) | 2008-09-18 | 2011-04-05 | Astellas Pharma Inc | Compuestos heterociclicos de carboxamida. |
| DK2593452T3 (en) | 2010-07-14 | 2017-04-24 | Novartis Ag | Heterocyclic compounds as IP receptor agonists |
| CN105026387B (zh) | 2013-01-29 | 2018-06-08 | Redx制药公开有限公司 | 作为软rock抑制剂的吡啶衍生物 |
| PL3573987T3 (pl) * | 2017-01-30 | 2021-08-30 | Chiesi Farmaceutici S.P.A. | Pochodne amidu tyrozynowego jako inhibitory kinazy Rho |
-
2019
- 2019-06-10 AR ARP190101592A patent/AR114926A1/es unknown
- 2019-06-11 MA MA052891A patent/MA52891A/fr unknown
- 2019-06-11 EP EP19735488.9A patent/EP3807273B1/en active Active
- 2019-06-11 US US16/973,514 patent/US20210253568A1/en not_active Abandoned
- 2019-06-11 WO PCT/EP2019/065119 patent/WO2019238628A1/en not_active Ceased
Also Published As
| Publication number | Publication date |
|---|---|
| EP3807273A1 (en) | 2021-04-21 |
| US20210253568A1 (en) | 2021-08-19 |
| MA52891A (fr) | 2021-04-28 |
| EP3807273B1 (en) | 2022-08-03 |
| WO2019238628A1 (en) | 2019-12-19 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FB | Suspension of granting procedure |