MX2019005526A - Derivados biciclicos de dihidropirimidina-carboxamida como inhibidores de rho-cinasa. - Google Patents
Derivados biciclicos de dihidropirimidina-carboxamida como inhibidores de rho-cinasa.Info
- Publication number
- MX2019005526A MX2019005526A MX2019005526A MX2019005526A MX2019005526A MX 2019005526 A MX2019005526 A MX 2019005526A MX 2019005526 A MX2019005526 A MX 2019005526A MX 2019005526 A MX2019005526 A MX 2019005526A MX 2019005526 A MX2019005526 A MX 2019005526A
- Authority
- MX
- Mexico
- Prior art keywords
- compounds
- carboxamide derivatives
- rho
- kinase inhibitors
- dihydropyrimidine
- Prior art date
Links
- 229940053202 antiepileptics carboxamide derivative Drugs 0.000 title abstract 2
- 125000002619 bicyclic group Chemical group 0.000 title abstract 2
- 239000003590 rho kinase inhibitor Substances 0.000 title 1
- 150000001875 compounds Chemical class 0.000 abstract 3
- 201000009794 Idiopathic Pulmonary Fibrosis Diseases 0.000 abstract 2
- 206010064911 Pulmonary arterial hypertension Diseases 0.000 abstract 2
- 208000036971 interstitial lung disease 2 Diseases 0.000 abstract 2
- 208000006545 Chronic Obstructive Pulmonary Disease Diseases 0.000 abstract 1
- 102000004190 Enzymes Human genes 0.000 abstract 1
- 108090000790 Enzymes Proteins 0.000 abstract 1
- 208000019693 Lung disease Diseases 0.000 abstract 1
- 208000006673 asthma Diseases 0.000 abstract 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 abstract 1
- 208000035475 disorder Diseases 0.000 abstract 1
- 230000002401 inhibitory effect Effects 0.000 abstract 1
- 230000007246 mechanism Effects 0.000 abstract 1
- 239000008194 pharmaceutical composition Substances 0.000 abstract 1
- 102000000568 rho-Associated Kinases Human genes 0.000 abstract 1
- 108010041788 rho-Associated Kinases Proteins 0.000 abstract 1
- 239000011435 rock Substances 0.000 abstract 1
- 230000001225 therapeutic effect Effects 0.000 abstract 1
Classifications
-
- 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)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (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)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Epidemiology (AREA)
- Immunology (AREA)
- Otolaryngology (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
- Medicinal Preparation (AREA)
- Plural Heterocyclic Compounds (AREA)
Abstract
La invención se relaciona con compuestos de fórmula (I) que inhiben Rho cinasa que son derivados de dihidro pirimidina-carboxamida bicíclicos, métodos para la preparación de los compuestos, composiciones farmacéuticas que los contienen y usos terapéuticos de los mismos. Particularmente, los compuestos de la invención pueden ser útiles en el tratamiento de muchos trastornos asociados con mecanismos de enzimas ROCK, como por ejemplo enfermedades pulmonares que incluyen asma, enfermedad pulmonar obstructiva crónica (COPD), fibrosis pulmonar idiopática (IPF) e hipertensión arterial pulmonar (PAH).
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP16205661 | 2016-12-21 | ||
| PCT/EP2017/084271 WO2018115383A1 (en) | 2016-12-21 | 2017-12-21 | Bicyclic dihydropyrimidine-carboxamide derivatives as rho-kinase inhibitors |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| MX2019005526A true MX2019005526A (es) | 2019-08-12 |
Family
ID=57583050
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| MX2019005526A MX2019005526A (es) | 2016-12-21 | 2017-12-21 | Derivados biciclicos de dihidropirimidina-carboxamida como inhibidores de rho-cinasa. |
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 |
|---|---|---|---|---|
| EP3710008A4 (en) | 2017-11-14 | 2021-08-25 | The Schepens Eye Research Institute, Inc. | RUNX1 INHIBITION FOR THE TREATMENT OF PROLIFERATIVE VITREORETINOPATHY AND DISEASES ASSOCIATED WITH EPITHELIAL-MESENCHYMAL TRANSITION |
| MA51283A (fr) | 2017-12-18 | 2021-05-26 | Chiesi Farm Spa | Dérivés de tyrosine en tant qu'inhibiteurs de kinase rho |
| AR113947A1 (es) | 2017-12-18 | 2020-07-01 | Chiesi Farm Spa | Derivados de azaindol como inhibidores de rho-quinasa |
| WO2019121233A1 (en) | 2017-12-18 | 2019-06-27 | Chiesi Farmaceutici S.P.A. | Oxadiazole derivatives as rho-kinase inhibitors |
| 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 |
| CA3110661A1 (en) | 2018-08-29 | 2020-03-05 | University Of Massachusetts | Inhibition of protein kinases to treat friedreich ataxia |
| EP3992183A4 (en) * | 2019-06-25 | 2023-06-21 | Beijing Tide Pharmaceutical Co., Ltd. | METHOD FOR THE TREATMENT OF IDIOPATHIC PULMONARY FIBROSIS |
| US11427558B1 (en) | 2019-07-11 | 2022-08-30 | ESCAPE Bio, Inc. | Indazoles and azaindazoles as LRRK2 inhibitors |
| US11858940B2 (en) | 2020-03-21 | 2024-01-02 | 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 |
| EP4263546B1 (en) | 2020-12-15 | 2025-07-02 | Chiesi Farmaceutici S.p.A. | Dihydrofuropyridine derivatives as rho- kinase inhibitors |
| IL303641A (en) | 2020-12-15 | 2023-08-01 | Chiesi Farm Spa | Dihydrofuropyridine derivatives as rho- kinase inhibitors |
| KR20230121812A (ko) | 2020-12-15 | 2023-08-21 | 키에시 파르마슈티시 엣스. 피. 에이. | Rho-키나아제 억제제로서 다이하이드로퓨로피리딘 유도체 |
| 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 |
| US20250000083A1 (en) | 2021-11-11 | 2025-01-02 | The Doshisha | 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 |
| US20080125427A1 (en) | 2004-06-17 | 2008-05-29 | Smithkline Beecham Corporation | Novel Inhibitors of Rho-Kinases |
| BRPI0710107A2 (pt) | 2006-03-30 | 2011-08-02 | Irm Llc | composto, composição compreendendo o mesmo, bem como uso do mesmo |
| CN101925603B (zh) | 2007-12-13 | 2013-12-04 | 沃泰克斯药物股份有限公司 | 囊性纤维化跨膜通道调节因子的调节剂 |
| CA2709918A1 (en) | 2007-12-21 | 2009-06-25 | 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 |
| EP2268641B1 (en) | 2008-03-26 | 2014-09-03 | Advinus Therapeutics Pvt. Ltd. | Heterocyclic compounds as adenosine receptor antagonist |
| JP2012502882A (ja) | 2008-09-18 | 2012-02-02 | アステラス製薬株式会社 | 複素環カルボキサミド化合物 |
| PL2593452T3 (pl) | 2010-07-14 | 2017-07-31 | Novartis Ag | Związki heterocykliczne będące agonistami receptora IP |
| 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 |
| KR102275616B1 (ko) | 2013-01-29 | 2021-07-09 | 레드엑스 파마 피엘씨 | 연성 rock 저해제로서 피리딘 유도체 |
| PT3811943T (pt) * | 2013-03-15 | 2023-03-15 | Aerie Pharmaceuticals Inc | Composto para uso no tratamento de distúrbios oculares |
| 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 AR ARP170103583A patent/AR110401A1/es not_active Application Discontinuation
- 2017-12-19 TW TW106144601A patent/TWI800498B/zh active
- 2017-12-21 BR BR112019012927-8A patent/BR112019012927A2/pt not_active Application Discontinuation
- 2017-12-21 MA MA047086A patent/MA47086A/fr unknown
- 2017-12-21 CA CA3039754A patent/CA3039754A1/en active Pending
- 2017-12-21 MX MX2019005526A patent/MX2019005526A/es unknown
- 2017-12-21 EP EP17828752.0A patent/EP3558999A1/en not_active Withdrawn
- 2017-12-21 CN CN201780076656.3A patent/CN110062758B/zh not_active Expired - Fee Related
- 2017-12-21 US US15/850,720 patent/US10584128B2/en active Active
- 2017-12-21 WO PCT/EP2017/084271 patent/WO2018115383A1/en not_active Ceased
- 2017-12-21 JP JP2019527305A patent/JP7090610B2/ja active Active
- 2017-12-21 KR KR1020197017094A patent/KR102559612B1/ko active Active
- 2017-12-21 AU AU2017382029A patent/AU2017382029B2/en not_active Ceased
Also Published As
| Publication number | Publication date |
|---|---|
| US20180170939A1 (en) | 2018-06-21 |
| RU2019121944A3 (es) | 2021-04-01 |
| CA3039754A1 (en) | 2018-06-28 |
| TWI800498B (zh) | 2023-05-01 |
| TW201829411A (zh) | 2018-08-16 |
| AU2017382029B2 (en) | 2022-02-17 |
| CN110062758B (zh) | 2023-01-17 |
| AU2017382029A1 (en) | 2019-05-30 |
| MA47086A (fr) | 2021-04-28 |
| CN110062758A (zh) | 2019-07-26 |
| KR20190092439A (ko) | 2019-08-07 |
| KR102559612B1 (ko) | 2023-07-26 |
| AR110401A1 (es) | 2019-03-27 |
| EP3558999A1 (en) | 2019-10-30 |
| BR112019012927A2 (pt) | 2020-02-18 |
| US10584128B2 (en) | 2020-03-10 |
| RU2019121944A (ru) | 2021-01-22 |
| JP7090610B2 (ja) | 2022-06-24 |
| WO2018115383A1 (en) | 2018-06-28 |
| JP2020503264A (ja) | 2020-01-30 |
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