BRPI0816554B8 - compostos como antagonistas de receptores de adenosina a1 - Google Patents
compostos como antagonistas de receptores de adenosina a1Info
- Publication number
- BRPI0816554B8 BRPI0816554B8 BRPI0816554A BRPI0816554A BRPI0816554B8 BR PI0816554 B8 BRPI0816554 B8 BR PI0816554B8 BR PI0816554 A BRPI0816554 A BR PI0816554A BR PI0816554 A BRPI0816554 A BR PI0816554A BR PI0816554 B8 BRPI0816554 B8 BR PI0816554B8
- Authority
- BR
- Brazil
- Prior art keywords
- optionally substituted
- straight
- cooh
- substituted
- group
- Prior art date
Links
- 150000001875 compounds Chemical class 0.000 title abstract 3
- OIRDTQYFTABQOQ-KQYNXXCUSA-N adenosine Chemical compound C1=NC=2C(N)=NC=NC=2N1[C@@H]1O[C@H](CO)[C@@H](O)[C@H]1O OIRDTQYFTABQOQ-KQYNXXCUSA-N 0.000 title 2
- 239000002126 C01EB10 - Adenosine Substances 0.000 title 1
- 229960005305 adenosine Drugs 0.000 title 1
- 239000002464 receptor antagonist Substances 0.000 title 1
- 229940044551 receptor antagonist Drugs 0.000 title 1
- 125000005843 halogen group Chemical group 0.000 abstract 4
- 125000000217 alkyl group Chemical group 0.000 abstract 3
- 125000000753 cycloalkyl group Chemical group 0.000 abstract 2
- 101150007969 ADORA1 gene Proteins 0.000 abstract 1
- XFXPMWWXUTWYJX-UHFFFAOYSA-N Cyanide Chemical group N#[C-] XFXPMWWXUTWYJX-UHFFFAOYSA-N 0.000 abstract 1
- 229940121359 adenosine receptor antagonist Drugs 0.000 abstract 1
- 125000003545 alkoxy group Chemical group 0.000 abstract 1
- 125000005119 alkyl cycloalkyl group Chemical group 0.000 abstract 1
- 125000003118 aryl group Chemical group 0.000 abstract 1
- 125000002837 carbocyclic group Chemical group 0.000 abstract 1
- 125000001316 cycloalkyl alkyl group Chemical group 0.000 abstract 1
- 125000001072 heteroaryl group Chemical group 0.000 abstract 1
- 125000004435 hydrogen atom Chemical group [H]* 0.000 abstract 1
- 125000002887 hydroxy group Chemical group [H]O* 0.000 abstract 1
- 239000000296 purinergic P1 receptor antagonist Substances 0.000 abstract 1
- 125000001424 substituent group Chemical group 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
- A61K31/425—Thiazoles
- A61K31/426—1,3-Thiazoles
-
- 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
- A61P11/02—Nasal agents, e.g. decongestants
-
- 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
- A61P11/00—Drugs for disorders of the respiratory system
- A61P11/08—Bronchodilators
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P13/00—Drugs for disorders of the urinary system
- A61P13/12—Drugs for disorders of the urinary system of the kidneys
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
- A61P17/04—Antipruritics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P19/00—Drugs for skeletal disorders
- A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
-
- 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
- A61P25/22—Anxiolytics
-
- 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
- A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
-
- 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
- A61P37/08—Antiallergic agents
-
- 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
- A61P9/06—Antiarrhythmics
-
- 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
- C07D277/00—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings
- C07D277/02—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings
- C07D277/20—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
- C07D277/32—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
- C07D277/56—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
- C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
- C07D417/04—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Public Health (AREA)
- Life Sciences & Earth Sciences (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Pulmonology (AREA)
- Cardiology (AREA)
- Heart & Thoracic Surgery (AREA)
- Biomedical Technology (AREA)
- Neurosurgery (AREA)
- Neurology (AREA)
- Immunology (AREA)
- Dermatology (AREA)
- Urology & Nephrology (AREA)
- Epidemiology (AREA)
- Otolaryngology (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Rheumatology (AREA)
- Physical Education & Sports Medicine (AREA)
- Psychiatry (AREA)
- Hospice & Palliative Care (AREA)
- Vascular Medicine (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Saccharide Compounds (AREA)
- Thiazole And Isothizaole Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Plural Heterocyclic Compounds (AREA)
- Addition Polymer Or Copolymer, Post-Treatments, Or Chemical Modifications (AREA)
Abstract
Compostos como antagonistas de receptores de adenosina A1. Estes compostos correspondem à fórmula (I), onde: R1 representa um grupo de arila ou heteroarila opcionalmente substituído por um ou mais substituintes selecionados de um grupo composto por átomos de halogênio, retos ou ramificados, substituídos opcionalmente por aquila, cicloalquila, hidroxi inferior retos ou ramificados, opcionalmente substitídos opcionalmente substituídos por alcóxico, cianureto, ou -C02R', onde R' representa um átomo de hidrogênio ou um grupo de alquila inferior substituido opcionalmente, reto ou ramificad; R representa um grupo selecionado de: a) um grupo de alquila inferior reto ou ramificado substituído por um ou mais grupos carbocílicos; (-COOH) e opcionalmente substituído por um ou mais grupos carboxilicos (-COOH) e opcionalmente substituído por um ou mais átomos de halogênio b) um grupo de cicloalquila substituido por um ou mais grupos carboxilicos (-COOH) e opcionalmente substituído por um ou mais átomos de halogênio; c) um grupo de alquilacicloalquila ou cicloalquila alquila reto ou tamificado substituído por um ou mais grupos carboxílicos (-COOH) e opcionalmente por um mais átomos de halogênio. Fórmula (I)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| ES200702643 | 2007-10-02 | ||
| ES200702643A ES2331220B1 (es) | 2007-10-02 | 2007-10-02 | Nuevos compuestos como antagonistas de los receptores a1 de adenosina. |
| PCT/IB2008/002556 WO2009044250A1 (en) | 2007-10-02 | 2008-09-30 | New compounds as adenosine a1 receptor antagonists |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| BRPI0816554A2 BRPI0816554A2 (pt) | 2015-11-24 |
| BRPI0816554B1 BRPI0816554B1 (pt) | 2019-04-09 |
| BRPI0816554B8 true BRPI0816554B8 (pt) | 2022-08-30 |
Family
ID=40303525
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| BRPI0816554A BRPI0816554B8 (pt) | 2007-10-02 | 2008-09-30 | compostos como antagonistas de receptores de adenosina a1 |
Country Status (20)
| Country | Link |
|---|---|
| US (1) | US8410282B2 (pt) |
| EP (1) | EP2197860B1 (pt) |
| JP (1) | JP5463592B2 (pt) |
| KR (1) | KR101312198B1 (pt) |
| CN (1) | CN101835766B (pt) |
| AT (1) | ATE510829T1 (pt) |
| AU (1) | AU2008306553B2 (pt) |
| BR (1) | BRPI0816554B8 (pt) |
| CA (1) | CA2700526C (pt) |
| CY (1) | CY1112079T1 (pt) |
| DK (1) | DK2197860T3 (pt) |
| EA (1) | EA022473B1 (pt) |
| ES (2) | ES2331220B1 (pt) |
| HR (1) | HRP20110557T1 (pt) |
| MX (1) | MX2010003576A (pt) |
| PL (1) | PL2197860T3 (pt) |
| PT (1) | PT2197860E (pt) |
| SI (1) | SI2197860T1 (pt) |
| WO (1) | WO2009044250A1 (pt) |
| ZA (1) | ZA201002139B (pt) |
Families Citing this family (12)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2011076734A1 (en) * | 2009-12-21 | 2011-06-30 | Euroscreen S.A. | Compounds, pharmaceutical composition and methods for use in treating inflammatory diseases |
| US9518033B2 (en) | 2013-01-03 | 2016-12-13 | Council Of Scientific & Industrial Research | (4E)-4-(4-substituted benzylideneamino)-2,3-dihydro-3-substituted-2-thioxothiazole-5-carbonitriles as A2AR antagonist and process for preparation thereof |
| ES2634628T3 (es) | 2013-07-02 | 2017-09-28 | Bristol-Myers Squibb Company | Derivados tricíclicos de pirido-carboxamida como inhibidores ROCK |
| AR096788A1 (es) | 2013-07-02 | 2016-02-03 | Bristol Myers Squibb Co | Compuestos tricíclicos de carboxamida como inhibidores potentes de rock |
| ES2578363B1 (es) * | 2015-01-22 | 2017-01-31 | Palobiofarma, S.L. | Moduladores de los receptores A3 de adenosina |
| ES2676535B1 (es) * | 2017-01-20 | 2019-04-29 | Palobiofarma Sl | Moduladores de los receptores a3 de adenosina |
| JP6827124B2 (ja) | 2017-03-06 | 2021-02-10 | パロビオファルマ、ソシエダッド、リミターダPalobiofarma S.L | (1r,3s)−3−(5−シアノ−4−フェニル−1,3−チアゾール−2−イルカルバモイル)シクロペンタンカルボン酸のアミン塩 |
| CN107739350B (zh) * | 2017-09-26 | 2020-12-22 | 天津大学 | 一种合成2-氨基噻唑衍生物的方法 |
| EA202190558A1 (ru) | 2018-09-17 | 2022-02-03 | Янгчжин Фарм. Ко., Лтд. | Новые производные тиазола и их фармацевтически приемлемые соли |
| EP3882240A1 (en) | 2020-03-16 | 2021-09-22 | Palobiofarma, S.L. | Cocrystals of (1r,3s)-3-(5-cyano-4-phenyl-1,3-thiazol-2-ylcabamoyl)cyclopentane carboxylic acid |
| EP3957308A1 (en) * | 2020-08-21 | 2022-02-23 | Palobiofarma, S.L. | (1r,3s)-3-((5-cyano-4-phenylthiazol-2-yl)carbamoyl)cyclopentane-1-carboxylic acid and derivatives thereof for use in the treatment of airway diseases |
| CN119039300A (zh) * | 2024-08-29 | 2024-11-29 | 上海信诺维生物医药有限公司 | 吡唑并嘧啶类化合物的制备方法 |
Family Cites Families (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2003039451A2 (en) * | 2001-11-08 | 2003-05-15 | Fujisawa Pharmaceutical Co., Ltd. | Thiazole pyridazinones as adenosine antagonists |
| EP2314586B1 (en) * | 2002-01-18 | 2016-09-14 | Astellas Pharma Inc. | 2-Acylaminothiazole derivative or salt thereof |
| EP2460800A1 (en) * | 2006-03-08 | 2012-06-06 | Achillion Pharmaceuticals, Inc. | Substituted aminothiazole derivatives with anti-HCV activity |
| WO2007116106A1 (es) * | 2006-04-12 | 2007-10-18 | Palobiofarma, S.L. | Nuevos compuestos como antagonistas de los receptores a1 de adenosina |
-
2007
- 2007-10-02 ES ES200702643A patent/ES2331220B1/es not_active Expired - Fee Related
-
2008
- 2008-09-30 JP JP2010527561A patent/JP5463592B2/ja active Active
- 2008-09-30 PL PL08835072T patent/PL2197860T3/pl unknown
- 2008-09-30 KR KR1020107008768A patent/KR101312198B1/ko active Active
- 2008-09-30 AU AU2008306553A patent/AU2008306553B2/en not_active Ceased
- 2008-09-30 PT PT08835072T patent/PT2197860E/pt unknown
- 2008-09-30 SI SI200830350T patent/SI2197860T1/sl unknown
- 2008-09-30 ES ES08835072T patent/ES2366075T3/es active Active
- 2008-09-30 BR BRPI0816554A patent/BRPI0816554B8/pt active IP Right Grant
- 2008-09-30 MX MX2010003576A patent/MX2010003576A/es active IP Right Grant
- 2008-09-30 DK DK08835072.3T patent/DK2197860T3/da active
- 2008-09-30 WO PCT/IB2008/002556 patent/WO2009044250A1/en not_active Ceased
- 2008-09-30 EA EA201000393A patent/EA022473B1/ru not_active IP Right Cessation
- 2008-09-30 HR HR20110557T patent/HRP20110557T1/hr unknown
- 2008-09-30 CA CA2700526A patent/CA2700526C/en active Active
- 2008-09-30 CN CN2008801126777A patent/CN101835766B/zh active Active
- 2008-09-30 AT AT08835072T patent/ATE510829T1/de active
- 2008-09-30 EP EP08835072A patent/EP2197860B1/en active Active
- 2008-09-30 US US12/679,941 patent/US8410282B2/en active Active
-
2010
- 2010-03-25 ZA ZA2010/02139A patent/ZA201002139B/en unknown
-
2011
- 2011-08-22 CY CY20111100805T patent/CY1112079T1/el unknown
Also Published As
| Publication number | Publication date |
|---|---|
| CA2700526A1 (en) | 2009-04-09 |
| KR101312198B1 (ko) | 2013-09-27 |
| BRPI0816554A2 (pt) | 2015-11-24 |
| PL2197860T3 (pl) | 2011-09-30 |
| CN101835766A (zh) | 2010-09-15 |
| BRPI0816554B1 (pt) | 2019-04-09 |
| AU2008306553B2 (en) | 2011-06-09 |
| ES2331220A1 (es) | 2009-12-23 |
| ES2331220B1 (es) | 2010-09-23 |
| HRP20110557T1 (hr) | 2011-09-30 |
| PT2197860E (pt) | 2011-08-26 |
| ZA201002139B (en) | 2011-06-29 |
| ATE510829T1 (de) | 2011-06-15 |
| JP2010540615A (ja) | 2010-12-24 |
| CN101835766B (zh) | 2013-09-25 |
| SI2197860T1 (sl) | 2011-09-30 |
| CY1112079T1 (el) | 2015-11-04 |
| EP2197860B1 (en) | 2011-05-25 |
| MX2010003576A (es) | 2010-04-22 |
| CA2700526C (en) | 2014-03-18 |
| US20100311703A1 (en) | 2010-12-09 |
| AU2008306553A1 (en) | 2009-04-09 |
| EA201000393A1 (ru) | 2010-08-30 |
| EA022473B1 (ru) | 2016-01-29 |
| EP2197860A1 (en) | 2010-06-23 |
| ES2366075T3 (es) | 2011-10-17 |
| DK2197860T3 (da) | 2011-08-15 |
| JP5463592B2 (ja) | 2014-04-09 |
| KR20100058653A (ko) | 2010-06-03 |
| US8410282B2 (en) | 2013-04-02 |
| WO2009044250A1 (en) | 2009-04-09 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| B07D | Technical examination (opinion) related to article 229 of industrial property law [chapter 7.4 patent gazette] | ||
| B06F | Objections, documents and/or translations needed after an examination request according [chapter 6.6 patent gazette] | ||
| B07E | Notification of approval relating to section 229 industrial property law [chapter 7.5 patent gazette] | ||
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