BR112014026651A8 - derivados de imidazotiadiazol e de imidazopiridazina como inibidores do receptor ativado por proteases 4 (par4) para o tratamento de agregação plaquetária - Google Patents
derivados de imidazotiadiazol e de imidazopiridazina como inibidores do receptor ativado por proteases 4 (par4) para o tratamento de agregação plaquetáriaInfo
- Publication number
- BR112014026651A8 BR112014026651A8 BR112014026651A BR112014026651A BR112014026651A8 BR 112014026651 A8 BR112014026651 A8 BR 112014026651A8 BR 112014026651 A BR112014026651 A BR 112014026651A BR 112014026651 A BR112014026651 A BR 112014026651A BR 112014026651 A8 BR112014026651 A8 BR 112014026651A8
- Authority
- BR
- Brazil
- Prior art keywords
- inhibitors
- platelet aggregation
- par4
- treatment
- activated receptor
- Prior art date
Links
- 239000003112 inhibitor Substances 0.000 title abstract 3
- 208000010110 spontaneous platelet aggregation Diseases 0.000 title abstract 3
- 102100040853 PRKC apoptosis WT1 regulator protein Human genes 0.000 title abstract 2
- 101710162991 PRKC apoptosis WT1 regulator protein Proteins 0.000 title abstract 2
- 102000004885 Protease-activated receptor 4 Human genes 0.000 title abstract 2
- 108090001010 Protease-activated receptor 4 Proteins 0.000 title abstract 2
- 150000005233 imidazopyridazines Chemical class 0.000 title abstract 2
- BOXRDDIXJOUZLV-UHFFFAOYSA-N 2h-imidazo[4,5-d]thiadiazole Chemical class N1SC2=NC=NC2=N1 BOXRDDIXJOUZLV-UHFFFAOYSA-N 0.000 abstract 1
- 150000001875 compounds Chemical class 0.000 abstract 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 abstract 1
- 229940079593 drug Drugs 0.000 abstract 1
- 239000003814 drug Substances 0.000 abstract 1
- 150000002148 esters Chemical class 0.000 abstract 1
- 229940002612 prodrug Drugs 0.000 abstract 1
- 239000000651 prodrug Substances 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 239000012453 solvate Substances 0.000 abstract 1
- 230000009424 thromboembolic effect Effects 0.000 abstract 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D513/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00
- C07D513/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00 in which the condensed system contains two hetero rings
- C07D513/04—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
- A61K31/41—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
- A61K31/433—Thidiazoles
-
- 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
- A61K31/4353—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 ortho- or peri-condensed with heterocyclic ring systems
- A61K31/437—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 ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
-
- 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
- A61K31/5375—1,4-Oxazines, e.g. morpholine
- A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K38/00—Medicinal preparations containing peptides
- A61K38/04—Peptides having up to 20 amino acids in a fully defined sequence; Derivatives thereof
- A61K38/12—Cyclic peptides, e.g. bacitracins; Polymyxins; Gramicidins S, C; Tyrocidins A, B or C
-
- 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
- A61P7/00—Drugs for disorders of the blood or the extracellular fluid
- A61P7/02—Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
-
- 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
-
- 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
- A61K31/435—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
- A61K31/4439—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
-
- 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
- A61K31/4965—Non-condensed pyrazines
- A61K31/497—Non-condensed pyrazines 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
- A61K31/513—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim having oxo groups directly attached to the heterocyclic ring, e.g. cytosine
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- Medicinal Chemistry (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Epidemiology (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Proteomics, Peptides & Aminoacids (AREA)
- Gastroenterology & Hepatology (AREA)
- Immunology (AREA)
- Hematology (AREA)
- Cardiology (AREA)
- Heart & Thoracic Surgery (AREA)
- Vascular Medicine (AREA)
- Urology & Nephrology (AREA)
- Diabetes (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
- Plural Heterocyclic Compounds (AREA)
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201261638567P | 2012-04-26 | 2012-04-26 | |
| PCT/US2013/037884 WO2013163241A1 (en) | 2012-04-26 | 2013-04-24 | Imidazothiadiazole and imidazopyridazine derivatives as protease activated receptor 4 (par4) inhibitors for treating platelet aggregation |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| BR112014026651A2 BR112014026651A2 (pt) | 2017-06-27 |
| BR112014026651A8 true BR112014026651A8 (pt) | 2018-01-16 |
Family
ID=48225151
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| BR112014026651A BR112014026651A8 (pt) | 2012-04-26 | 2013-04-24 | derivados de imidazotiadiazol e de imidazopiridazina como inibidores do receptor ativado por proteases 4 (par4) para o tratamento de agregação plaquetária |
Country Status (14)
| Country | Link |
|---|---|
| US (1) | US9518064B2 (https=) |
| EP (1) | EP2855489B1 (https=) |
| JP (1) | JP6101343B2 (https=) |
| KR (1) | KR20150003766A (https=) |
| CN (1) | CN104640869B (https=) |
| AU (1) | AU2013251680A1 (https=) |
| BR (1) | BR112014026651A8 (https=) |
| CA (1) | CA2871599A1 (https=) |
| EA (1) | EA201491954A1 (https=) |
| ES (1) | ES2617879T3 (https=) |
| IL (1) | IL235141A0 (https=) |
| MX (1) | MX2014012741A (https=) |
| SG (1) | SG11201406733QA (https=) |
| WO (1) | WO2013163241A1 (https=) |
Families Citing this family (24)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| SI2841437T1 (sl) | 2012-04-26 | 2017-09-29 | Bristol-Myers Squibb Company | Derivati imidazotiadiazola in imidazopirazina kot proteazno aktivirani receptor 4 (PAR4) inhibitorji za zdravljenje agregacije trombocitov |
| SG11201406759YA (en) * | 2012-04-26 | 2014-11-27 | Bristol Myers Squibb Co | Imidazothiadiazole derivatives as protease activated receptor 4 (par4) inhibitors for treating platelet aggregation |
| WO2015124570A1 (en) | 2014-02-18 | 2015-08-27 | INSERM (Institut National de la Santé et de la Recherche Médicale) | Methods and pharmaceutical composition for the treatment of influenza a virus infection |
| PE20161176A1 (es) | 2014-03-24 | 2016-11-19 | Bayer Cropscience Ag | Derivados de fenilpiperidincarboxamida como fungicidas |
| US9617279B1 (en) | 2014-06-24 | 2017-04-11 | Bristol-Myers Squibb Company | Imidazooxadiazole compounds |
| US9598419B1 (en) | 2014-06-24 | 2017-03-21 | Universite De Montreal | Imidazotriazine and imidazodiazine compounds |
| EP3262052A1 (en) | 2015-02-26 | 2018-01-03 | Bristol-Myers Squibb Company | Benzothiazole and benzothiophne compounds |
| WO2016134450A1 (en) | 2015-02-26 | 2016-09-01 | Université de Montréal | Imidazopyridazine and imidazothiadiazole compounds |
| US9789087B2 (en) * | 2015-08-03 | 2017-10-17 | Thomas Jefferson University | PAR4 inhibitor therapy for patients with PAR4 polymorphism |
| EP3371196B1 (en) | 2015-10-19 | 2021-10-27 | Université de Montréal | Heterocyclic compounds as inhibitors of platelet aggregation |
| WO2017184520A1 (en) * | 2016-04-18 | 2017-10-26 | Vanderbilt University | Substituted and fused 6-membered protease activated receptor 4 (par-4) antagonists |
| EP3484878B1 (en) | 2016-07-14 | 2020-08-19 | Bristol-Myers Squibb Company | Bicyclic heteroaryl substituted compounds |
| KR102494647B1 (ko) | 2016-07-14 | 2023-01-31 | 브리스톨-마이어스 스큅 컴퍼니 | 비시클릭 헤테로아릴 치환된 화합물 |
| CN109689642B (zh) | 2016-07-14 | 2022-04-12 | 百时美施贵宝公司 | 经单环杂芳基取代的化合物 |
| CN109689664B (zh) * | 2016-07-14 | 2022-04-15 | 百时美施贵宝公司 | 作为par4抑制剂的三环杂芳基取代的喹啉和氮杂喹啉化合物 |
| ES2926580T3 (es) * | 2016-12-23 | 2022-10-27 | Minoryx Therapeutics S L | Proceso para preparar 5-[[4-[2-[5-(1-hidroxietil)-2-piridinil]etoxi]fenil]metil]-2,4-tiazolidindiona y sales de la misma |
| CN111094300B (zh) * | 2018-01-31 | 2022-09-16 | 江苏恒瑞医药股份有限公司 | 苯并杂芳基类衍生物、其制备方法及其在医药上的应用 |
| CN110218218B (zh) * | 2018-03-01 | 2022-04-08 | 江苏恒瑞医药股份有限公司 | 苯并呋喃类衍生物、其制备方法及其在医药上的应用 |
| CN112074522B (zh) * | 2018-05-16 | 2022-08-26 | 深圳信立泰药业股份有限公司 | 作为用于治疗血小板聚集的蛋白酶激活受体4(par4)抑制剂的化合物 |
| WO2019218955A1 (zh) * | 2018-05-16 | 2019-11-21 | 深圳信立泰药业股份有限公司 | 作为用于治疗血小板聚集的蛋白酶激活受体4(par4)抑制剂的化合物 |
| CN110627817B (zh) * | 2018-06-25 | 2022-03-29 | 中国药科大学 | 咪唑并环类par4拮抗剂及其医药用途 |
| CN111349105B (zh) * | 2018-12-24 | 2023-04-07 | 江苏恒瑞医药股份有限公司 | 苯并呋喃类衍生物、其制备方法及其在医药上的应用 |
| CN109651126A (zh) * | 2019-01-17 | 2019-04-19 | 杭州师范大学 | 一种四苯乙烯基羧酸有机配体及其配合物的制备方法 |
| CN113150005B (zh) * | 2021-04-09 | 2022-08-30 | 中国药科大学 | 喹喔啉类化合物、制备方法及其在医药上的应用 |
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| AU2009231906A1 (en) | 2008-03-31 | 2009-10-08 | Metabolex, Inc. | Oxymethylene aryl compounds and uses thereof |
| US9006252B2 (en) | 2008-09-26 | 2015-04-14 | National Health Research Institutes | Fused multicyclic compounds as protein kinase inhibitors |
| SG172352A1 (en) | 2008-12-23 | 2011-07-28 | Abbott Lab | Anti-viral compounds |
| FR2948521B1 (fr) | 2009-07-21 | 2012-01-27 | Dxo Labs | Procede d'estimation d'un defaut d'un systeme de capture d'images et systemes associes |
| WO2011074658A1 (ja) | 2009-12-18 | 2011-06-23 | 田辺三菱製薬株式会社 | 新規抗血小板薬 |
| CN102372701A (zh) | 2010-08-10 | 2012-03-14 | 江苏恒瑞医药股份有限公司 | 氮杂双环己烷类衍生物、其制备方法及其在医药上的应用 |
| TW201217365A (en) | 2010-08-11 | 2012-05-01 | Millennium Pharm Inc | Heteroaryls and uses thereof |
| CN103874496A (zh) | 2011-08-22 | 2014-06-18 | 默沙东公司 | 作为bace抑制剂的2-螺-取代的亚氨基噻嗪类及其单和二氧化物、组合物及其用途 |
| SI2841437T1 (sl) | 2012-04-26 | 2017-09-29 | Bristol-Myers Squibb Company | Derivati imidazotiadiazola in imidazopirazina kot proteazno aktivirani receptor 4 (PAR4) inhibitorji za zdravljenje agregacije trombocitov |
| SG11201406759YA (en) | 2012-04-26 | 2014-11-27 | Bristol Myers Squibb Co | Imidazothiadiazole derivatives as protease activated receptor 4 (par4) inhibitors for treating platelet aggregation |
| US9605002B2 (en) | 2012-07-18 | 2017-03-28 | University Of Notre Dame Du Lac | 5,5-heteroaromatic anti-infective compounds |
-
2013
- 2013-04-24 EP EP13719360.3A patent/EP2855489B1/en active Active
- 2013-04-24 US US14/396,831 patent/US9518064B2/en active Active
- 2013-04-24 JP JP2015509093A patent/JP6101343B2/ja active Active
- 2013-04-24 BR BR112014026651A patent/BR112014026651A8/pt not_active IP Right Cessation
- 2013-04-24 SG SG11201406733QA patent/SG11201406733QA/en unknown
- 2013-04-24 EA EA201491954A patent/EA201491954A1/ru unknown
- 2013-04-24 ES ES13719360.3T patent/ES2617879T3/es active Active
- 2013-04-24 MX MX2014012741A patent/MX2014012741A/es unknown
- 2013-04-24 CN CN201380033473.5A patent/CN104640869B/zh active Active
- 2013-04-24 WO PCT/US2013/037884 patent/WO2013163241A1/en not_active Ceased
- 2013-04-24 AU AU2013251680A patent/AU2013251680A1/en not_active Abandoned
- 2013-04-24 CA CA 2871599 patent/CA2871599A1/en not_active Abandoned
- 2013-04-24 KR KR20147030172A patent/KR20150003766A/ko not_active Withdrawn
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2014
- 2014-10-19 IL IL235141A patent/IL235141A0/en unknown
Also Published As
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|---|---|
| US20150119390A1 (en) | 2015-04-30 |
| IL235141A0 (en) | 2014-12-31 |
| MX2014012741A (es) | 2015-04-13 |
| US9518064B2 (en) | 2016-12-13 |
| BR112014026651A2 (pt) | 2017-06-27 |
| CN104640869A (zh) | 2015-05-20 |
| AU2013251680A1 (en) | 2014-11-13 |
| WO2013163241A1 (en) | 2013-10-31 |
| JP6101343B2 (ja) | 2017-03-22 |
| EP2855489A1 (en) | 2015-04-08 |
| KR20150003766A (ko) | 2015-01-09 |
| JP2015514806A (ja) | 2015-05-21 |
| CA2871599A1 (en) | 2013-10-31 |
| ES2617879T3 (es) | 2017-06-20 |
| SG11201406733QA (en) | 2014-11-27 |
| EP2855489B1 (en) | 2017-01-04 |
| CN104640869B (zh) | 2017-12-12 |
| EA201491954A1 (ru) | 2015-01-30 |
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