AR110401A1 - Derivados dihidropirimidina bicíclica-carboxamida como inhibidores de rho-quinasa - Google Patents
Derivados dihidropirimidina bicíclica-carboxamida como inhibidores de rho-quinasaInfo
- Publication number
- AR110401A1 AR110401A1 ARP170103583A ARP170103583A AR110401A1 AR 110401 A1 AR110401 A1 AR 110401A1 AR P170103583 A ARP170103583 A AR P170103583A AR P170103583 A ARP170103583 A AR P170103583A AR 110401 A1 AR110401 A1 AR 110401A1
- Authority
- AR
- Argentina
- Prior art keywords
- alkyl
- heterocycloalkyl
- alkoxy
- aryl
- heteroaryl
- Prior art date
Links
Classifications
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- 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
-
- 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
- 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
-
- 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
-
- 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
-
- 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
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Pulmonology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Epidemiology (AREA)
- Immunology (AREA)
- Otolaryngology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
- Medicinal Preparation (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Plural Heterocyclic Compounds (AREA)
Abstract
Reivindicación 1: Un compuesto caracterizado porque es de fórmula (1), donde X¹ y X² son en cada caso en forma independiente un átomo de carbono o un átomo de nitrógeno; cada R, cuando está presente, se selecciona en cada caso en forma independiente del grupo que consiste en -H, -CN, halógeno, -NR⁵R⁶, C₁₋₆ alquilo, C₁₋₆ haloalquilo, C₁₋₆ hidroxialquilo, C₁₋₆ aminoalquilo, C₃₋₁₀ cicloalquilo, C₂₋₆ alquenilo, C₅₋₇ cicloalquenilo, C₂₋₆ alquinilo, C₂₋₆ hidroxialquinilo, hidroxicarbonilo, -OR⁷, C₁₋₆ alquiltio, C₁₋₆ alcoxi-C₁₋₆ alquilo, C₁₋₆ alcoxicarbonilo, C₁₋₆ aminoalquilcarbonilo, carbamoílo, C₃₋₆ cicloalquil-C₁₋₆ alquilo, C₃₋₆ heterocicloalquil-C₁₋₆ alquilo, arilo, heteroarilo y C₃₋₆ heterocicloalquilo; donde cualquiera de dichos C₃₋₆ cicloalquilo, arilo, heteroarilo y C₃₋₆ heterocicloalquilo está a su vez opcionalmente sustituido en forma independiente con uno o más grupos seleccionados entre halógeno, -OH, C₁₋₆ alquilo, C₁₋₆ haloalquilo, C₁₋₆ hidroxialquilo, C₁₋₆ aminoalquilo, C₃₋₁₀ cicloalquilo, C₂₋₆ alquenilo, C₅₋₇ cicloalquenilo, C₂₋₆ alquinilo, C₂₋₆ hidroxialquinilo, C₁₋₆ alcoxilo, C₁₋₆ aminoalquilcarbonilo; R⁵ y R⁶ se seleccionan en cada caso en forma independiente del grupo H, C₁₋₆ alquilo, C₁₋₆ haloalquilo, C₁₋₆ hidroxialquilo, C₁₋₆ aminoalquilo, C₁₋₆ alcoxilo, C₁₋₆ alcoxi-C₁₋₆ alquilo, C₃₋₆ heterocicloalquil-C₁₋₆ alquilo, C₃₋₆ heterocicloalquiloxilo, alcanoilo, arilo, heteroarilo y C₃₋₆ heterocicloalquilo; donde cualquiera de dichos arilo, heteroarilo y C₃₋₆ heterocicloalquilo está a su vez opcionalmente sustituido en forma independiente con uno o más grupos seleccionados entre halógeno, -OH, C₁₋₆ alquilo; o R⁵ y R⁶ tomados juntos con el átomo de nitrógeno se unen para formar un radical heterocíclico de 4 a 6 miembros, donde al menos un átomo de carbono adicional del anillo en dicho radical heterocíclico se puede reemplazar por al menos un heteroátomo seleccionado entre N, S ó O; dicho radical heterocíclico puede estar además opcionalmente sustituido con un grupo seleccionado entre H, -CN, halógeno, -oxo, -NR⁵R⁶, C₁₋₆ alquilo, C₁₋₆ haloalquilo, C₁₋₆ hidroxialquilo, C₁₋₆ aminoalquilo, C₁₋₆ alcoxilo, C₁₋₆ alcoxi-C₁₋₆ alquilo, alcanoilo; R⁷ se selecciona en cada caso en forma independiente entre el grupo H, C₁₋₆ alquilo, C₁₋₆ haloalquilo, C₁₋₆ hidroxialquilo, C₁₋₆ aminoalquilo, C₁₋₆ alcoxi-C₁₋₆ alquilo, C₃₋₆ heterocicloalquil-C₁₋₆ alquilo, arilo, heteroarilo y C₃₋₆ heterocicloalquilo; donde cualquiera de dichos arilo, heteroarilo y C₃₋₆ heterocicloalquilo está a su vez opcionalmente sustituido en forma independiente con uno o más grupos seleccionados entre halógeno, -OH, C₁₋₆ alquilo; p es 0, 1 ó 2; R¹ se selecciona entre el grupo que consiste en C₁₋₆ alquilo, C₁₋₆ haloalquilo, C₁₋₆ hidroxialquilo, C₁₋₆ aminoalquilo, C₃₋₁₀ cicloalquilo, C₂₋₆ alquenilo, C₅₋₇ cicloalquenilo, C₂₋₆ alquinilo, C₂₋₆ hidroxialquinilo, C₃₋₆ cicloalquil-C₁₋₆ alquilo, C₃₋₆ heterocicloalquil-C₁₋₆ alquilo, arilo-C₁₋₆ alquilo, arilo, heteroarilo y C₃₋₆ heterocicloalquilo; donde cada uno de dichos cicloalquilo, cicloalquenilo, arilo, heteroarilo y C₃₋₆ heterocicloalquilo está a su vez opcionalmente sustituido en forma independiente con uno o más grupos seleccionados entre nitro, halógeno, -NR⁵R⁶, -CN, -OH, -S(O)₂-C₁₋₆ alquilo, C₁₋₆ alquilo, C₁₋₆ haloalquilo, C₁₋₆ alcoxilo, C₁₋₆ haloalcoxilo, C₁₋₆ aminoalcoxilo, C₁₋₆ hidroxialcoxilo, C₃₋₆ heterocicloalquiloxilo, C₃₋₆ heterocicloalquilo, C₁₋₆ alcoxilo, carbamoílo, alcanoilo, ariloxilo, arilo, C₁₋₆ alcoxilo, ariloxi-C₁₋₆ alquilo, C₁₋₆ alcoxicarbonilo, C₁₋₆ alcoxi-C₁₋₆ alquilo, C₁₋₆ alcoxicarbonil-amino-, C₁₋₆ hidroxialquilo, C₂₋₆ alquenilo, C₂₋₆ alquinilo, C₂₋₆ hidroxialquinilo, arilo, heteroarilo y C₃₋₆ heterocicloalquilo; R² se selecciona entre C₁₋₆ alquilo, C₁₋₆ haloalquilo, C₁₋₆ hidroxialquilo, C₁₋₆ aminoalquilo, C₃₋₁₀ cicloalquilo, C₁₋₆ alcoxilo, C₁₋₆ alcoxi-C₁₋₆ alquilo; A es un heteroarilo bicíclico opcionalmente sustituido con uno o más grupos seleccionados entre halógeno, OH, C₁₋₆ alquilo, C₁₋₆ alcoxilo, C₂₋₆ alquenilo, C₂₋₆ alquinilo, arilo, heteroarilo y C₃₋₆ heterocicloalquilo; donde cada uno de dichos arilo, heteroarilo y C₃₋₆ heterocicloalquilo está a su vez opcionalmente sustituido; o sus sales aceptables farmacéuticamente y solvatos.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP16205661 | 2016-12-21 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR110401A1 true AR110401A1 (es) | 2019-03-27 |
Family
ID=57583050
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP170103583A AR110401A1 (es) | 2016-12-21 | 2017-12-19 | Derivados dihidropirimidina bicíclica-carboxamida como inhibidores de rho-quinasa |
Country Status (13)
| Country | Link |
|---|---|
| US (1) | US10584128B2 (es) |
| EP (1) | EP3558999A1 (es) |
| JP (1) | JP7090610B2 (es) |
| KR (1) | KR102559612B1 (es) |
| CN (1) | CN110062758B (es) |
| AR (1) | AR110401A1 (es) |
| AU (1) | AU2017382029B2 (es) |
| BR (1) | BR112019012927A2 (es) |
| CA (1) | CA3039754A1 (es) |
| MA (1) | MA47086A (es) |
| MX (1) | MX2019005526A (es) |
| TW (1) | TWI800498B (es) |
| WO (1) | WO2018115383A1 (es) |
Families Citing this family (17)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CA3082643A1 (en) | 2017-11-14 | 2019-05-23 | The Schepens Eye Research Institute, Inc. | Runx1 inhibition for treatment of proliferative vitreoretinopathy and conditions associated with epithelial to mesenchymal transition |
| US11578068B2 (en) | 2017-12-18 | 2023-02-14 | Chiesi Farmaceutici S.P.A. | Oxadiazole derivatives as Rho-Kinase Inhibitors |
| EP3728246B1 (en) | 2017-12-18 | 2021-09-22 | Chiesi Farmaceutici S.p.A. | Meta tyrosine derivatives as rho-kinase inhibitors |
| MA51285A (fr) | 2017-12-18 | 2021-04-28 | Chiesi Farm Spa | Dérivés d'azaindole comme inhibiteurs de rho-kinase |
| WO2019222173A1 (en) * | 2018-05-15 | 2019-11-21 | E-Scape Bio, Inc. | Fused tetrazoles as lrrk2 inhibitors |
| TW202019923A (zh) | 2018-07-16 | 2020-06-01 | 義大利商吉斯藥品公司 | 作為Ｒｈｏ－激酶抑制劑之酪胺酸醯胺衍生物 |
| US12281308B2 (en) | 2018-08-29 | 2025-04-22 | University Of Massachusetts | Inhibition of protein kinases to treat Friedreich ataxia |
| CA3144113A1 (en) * | 2019-06-25 | 2020-12-30 | Beijing Tide Pharmaceutical Co., Ltd. | Method for treating idiopathic pulmonary fibrosis |
| WO2021007477A1 (en) | 2019-07-11 | 2021-01-14 | E-Scape Bio, Inc. | Indazoles and azaindazoles as lrrk2 inhibitors |
| EP4121167A1 (en) * | 2020-03-21 | 2023-01-25 | Arvinas Operations, Inc. | Selective modulators of mutant lrrk2 proteolysis and associated methods of use |
| CN111333655B (zh) * | 2020-04-13 | 2021-07-13 | 武汉工程大学 | 一种三唑并嘧啶类化合物及其制备方法和应用 |
| 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 |
| ES3041795T3 (en) | 2020-12-15 | 2025-11-14 | Chiesi Farm Spa | Dihydrofuropyridine derivatives as rho- kinase inhibitors |
| CN112624911A (zh) * | 2021-01-15 | 2021-04-09 | 阿里生物新材料（常州）有限公司 | 一种2-氯-3-氟-4-（三氟甲基）苯甲醛及其合成方法 |
| AU2022385051A1 (en) | 2021-11-11 | 2024-06-20 | Actualeyes Inc. | Cryopreservation preparation for corneal endothelial cells and method for producing said cryopreservation preparation |
| WO2023110700A1 (en) | 2021-12-13 | 2023-06-22 | Chiesi Farmaceutici S.P.A. | Dihydrofuropyridine derivatives as rho-kinase inhibitors |
Family Cites Families (17)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| MY125533A (en) * | 1999-12-06 | 2006-08-30 | Bristol Myers Squibb Co | Heterocyclic dihydropyrimidine compounds |
| WO2004039796A1 (de) | 2002-10-28 | 2004-05-13 | Bayer Healthcare Ag | Heteroaryloxy-substituierte phenylaminopyrimidine als rho-kinaseinhibitoren |
| US7482356B2 (en) * | 2003-11-10 | 2009-01-27 | The Procter & Gamble Company | Bicyclic pyrazolone cytokine inhibitors |
| 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 |
| CA2645967C (en) * | 2006-03-30 | 2011-05-24 | Irm Llc | Compounds and compositions as inhibitors of cannabinoid receptor 1 activity |
| AU2008335031B2 (en) | 2007-12-13 | 2013-11-28 | Vertex Pharmaceuticals Incorporated | Modulators of cystic fibrosis transmembrane conductance regulator |
| US20110150833A1 (en) | 2007-12-21 | 2011-06-23 | The Scripps Research Institute | Benzopyrans and analogs as rho kinase inhibitors |
| CN101195626A (zh) * | 2007-12-26 | 2008-06-11 | 北京理工大学 | 一种合成吡唑并[3,4-d]嘧啶-4(5H)-酮类化合物的方法 |
| BRPI0909157A2 (pt) * | 2008-03-26 | 2015-11-24 | Advinus Therapeutics Private Ltd | compostos heterocíclicos como antagonistas de receptores de adenosina |
| 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 |
| US9487522B2 (en) * | 2011-03-18 | 2016-11-08 | The Regents Of The University Of California | SSH-2 (slingshot-2) inhibitors and methods for making and using them |
| CN103193780B (zh) * | 2012-04-24 | 2015-07-08 | 广州融新生物科技有限公司 | 4,7-二氢四唑[1,5-α]嘧啶类化合物及其衍生物在制备预防或治疗脑出血药物中的应用 |
| 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 |
| FI3811943T3 (fi) * | 2013-03-15 | 2023-04-14 | Aerie Pharmaceuticals Inc | Yhdiste käytettäväksi silmäsairauksien hoidossa |
| US20160113931A1 (en) | 2014-10-24 | 2016-04-28 | University Of Macau | Method of treating and/or preventing neurodegenerative diseases |
| US9687483B2 (en) | 2015-01-26 | 2017-06-27 | BioAxone BioSciences, Inc. | Treatment of cerebral cavernous malformations and cerebral aneurysms with Rho kinase inhibitors |
-
2017
- 2017-12-19 TW TW106144601A patent/TWI800498B/zh active
- 2017-12-19 AR ARP170103583A patent/AR110401A1/es not_active Application Discontinuation
- 2017-12-21 MX MX2019005526A patent/MX2019005526A/es unknown
- 2017-12-21 BR BR112019012927-8A patent/BR112019012927A2/pt not_active Application Discontinuation
- 2017-12-21 CN CN201780076656.3A patent/CN110062758B/zh not_active Expired - Fee Related
- 2017-12-21 JP JP2019527305A patent/JP7090610B2/ja active Active
- 2017-12-21 EP EP17828752.0A patent/EP3558999A1/en not_active Withdrawn
- 2017-12-21 WO PCT/EP2017/084271 patent/WO2018115383A1/en not_active Ceased
- 2017-12-21 AU AU2017382029A patent/AU2017382029B2/en not_active Ceased
- 2017-12-21 MA MA047086A patent/MA47086A/fr unknown
- 2017-12-21 US US15/850,720 patent/US10584128B2/en active Active
- 2017-12-21 CA CA3039754A patent/CA3039754A1/en active Pending
- 2017-12-21 KR KR1020197017094A patent/KR102559612B1/ko active Active
Also Published As
| Publication number | Publication date |
|---|---|
| KR20190092439A (ko) | 2019-08-07 |
| KR102559612B1 (ko) | 2023-07-26 |
| CN110062758B (zh) | 2023-01-17 |
| CA3039754A1 (en) | 2018-06-28 |
| CN110062758A (zh) | 2019-07-26 |
| AU2017382029A1 (en) | 2019-05-30 |
| RU2019121944A (ru) | 2021-01-22 |
| MA47086A (fr) | 2021-04-28 |
| EP3558999A1 (en) | 2019-10-30 |
| BR112019012927A2 (pt) | 2020-02-18 |
| JP7090610B2 (ja) | 2022-06-24 |
| AU2017382029B2 (en) | 2022-02-17 |
| MX2019005526A (es) | 2019-08-12 |
| WO2018115383A1 (en) | 2018-06-28 |
| TW201829411A (zh) | 2018-08-16 |
| TWI800498B (zh) | 2023-05-01 |
| JP2020503264A (ja) | 2020-01-30 |
| US20180170939A1 (en) | 2018-06-21 |
| RU2019121944A3 (es) | 2021-04-01 |
| US10584128B2 (en) | 2020-03-10 |
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