PE20170939A1 - Pirimidinonas como inhibidores del factor xia - Google Patents
Pirimidinonas como inhibidores del factor xiaInfo
- Publication number
- PE20170939A1 PE20170939A1 PE2017000527A PE2017000527A PE20170939A1 PE 20170939 A1 PE20170939 A1 PE 20170939A1 PE 2017000527 A PE2017000527 A PE 2017000527A PE 2017000527 A PE2017000527 A PE 2017000527A PE 20170939 A1 PE20170939 A1 PE 20170939A1
- Authority
- PE
- Peru
- Prior art keywords
- pyrimidinones
- inhibitors
- fxia
- chloro
- refers
- Prior art date
Links
Classifications
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- 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
- C07D471/12—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 three hetero rings
- C07D471/18—Bridged systems
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- 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
-
- 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
- A61K31/415—1,2-Diazoles
- A61K31/4162—1,2-Diazoles condensed with heterocyclic ring systems
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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
- A61K31/495—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
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- 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
- 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
- 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
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- 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
- A61P7/06—Antianaemics
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- 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
- A61P9/04—Inotropic agents, i.e. stimulants of cardiac contraction; Drugs for heart failure
-
- 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
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
- C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
- C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
- C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom 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
- C07D213/61—Halogen atoms or nitro radicals
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
- C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
- C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
- C07D239/28—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more 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, directly attached to ring carbon atoms
- C07D239/32—One oxygen, sulfur or nitrogen atom
- C07D239/34—One oxygen atom
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
- C07D403/10—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a carbon chain containing aromatic rings
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Cardiology (AREA)
- Heart & Thoracic Surgery (AREA)
- Hematology (AREA)
- Diabetes (AREA)
- Urology & Nephrology (AREA)
- Epidemiology (AREA)
- Hospice & Palliative Care (AREA)
- Pulmonology (AREA)
- Vascular Medicine (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)
Abstract
Se refiere a un derivado de pirimidinona de formula (I) donde A es un anillo de tipo a) o b); B es un anillo de tipo c) o d); R1 es H o alquilo C1-C4; R2 es H, F, entre otros; R3 es H, CHF2, entre otros; R4 es H o F; R5 es H, F, entre otros. Es un seleccionado: trifluoroacetato de (9R,13S)-13-{4-[5-cloro-2-(4-cloro-1H-1, 2, 3-triazol-1-il)fenil]-6-oxo-1, 6-dihidropirimidin-1-il}-3-(difluorometil)-9-metil-3, 4, 7, 15-tetraazatriciclo[12.3.1.02.6]octadeca-1(18), 2(6), 4, 14, 16-pentaen-8-ona; entre otros. Tambien se refiere a una composicion farmaceutica. Dicho compuesto es un inhibidor selectivo del factor de coagulacion XIa (FXIa) o inhibidor dual de FXIa y calicreina plasmatica, siendo util para el tratamiento de trastornos tromboembolicos y/o inflamatorios
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201462058316P | 2014-10-01 | 2014-10-01 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| PE20170939A1 true PE20170939A1 (es) | 2017-07-13 |
Family
ID=53784023
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| PE2020001966A PE20210922A1 (es) | 2014-10-01 | 2015-07-29 | Pirimidinonas como inhibidores del factor xia |
| PE2017000527A PE20170939A1 (es) | 2014-10-01 | 2015-07-29 | Pirimidinonas como inhibidores del factor xia |
Family Applications Before (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| PE2020001966A PE20210922A1 (es) | 2014-10-01 | 2015-07-29 | Pirimidinonas como inhibidores del factor xia |
Country Status (34)
| Country | Link |
|---|---|
| EP (4) | EP3089979B1 (es) |
| JP (4) | JP6462865B2 (es) |
| KR (2) | KR101921436B1 (es) |
| CN (3) | CN106795161B (es) |
| AR (1) | AR101367A1 (es) |
| AU (3) | AU2015324530B2 (es) |
| CA (1) | CA2963395C (es) |
| CL (1) | CL2017000712A1 (es) |
| CO (1) | CO2017003833A2 (es) |
| CY (2) | CY1119678T1 (es) |
| DK (2) | DK3089979T3 (es) |
| EA (1) | EA031590B1 (es) |
| ES (3) | ES2836270T3 (es) |
| HR (2) | HRP20171950T1 (es) |
| HU (2) | HUE038061T2 (es) |
| IL (2) | IL251434B (es) |
| LT (2) | LT3089979T (es) |
| MA (1) | MA40123A1 (es) |
| MX (2) | MX376056B (es) |
| MY (2) | MY183987A (es) |
| NO (1) | NO2721243T3 (es) |
| PE (2) | PE20210922A1 (es) |
| PH (2) | PH12017500580B1 (es) |
| PL (1) | PL3089979T3 (es) |
| PT (2) | PT3089979T (es) |
| RS (2) | RS56786B1 (es) |
| SG (2) | SG11201702576QA (es) |
| SI (2) | SI3089979T1 (es) |
| SM (2) | SMT202000667T1 (es) |
| TN (2) | TN2017000112A1 (es) |
| TW (3) | TWI834182B (es) |
| UY (1) | UY36244A (es) |
| WO (1) | WO2016053455A1 (es) |
| ZA (1) | ZA201702478B (es) |
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| GB201116559D0 (en) | 2011-09-26 | 2011-11-09 | Univ Leuven Kath | Novel viral replication inhibitors |
| NO2760821T3 (es) | 2014-01-31 | 2018-03-10 | ||
| BR112016015717B1 (pt) * | 2014-01-31 | 2023-04-04 | Bristol-Myers Squibb Company | Compostos macrociclos com grupos p2' heterocíclicos como inibidores do fator xia, composição farmacêutica compreendendo os referidos compostos e uso dos mesmos |
| JP6526796B2 (ja) | 2014-09-04 | 2019-06-05 | ブリストル−マイヤーズ スクイブ カンパニーＢｒｉｓｔｏｌ−Ｍｙｅｒｓ Ｓｑｕｉｂｂ Ｃｏｍｐａｎｙ | Ｆｘｉａ阻害剤であるジアミドマクロ環 |
| NO2721243T3 (es) * | 2014-10-01 | 2018-10-20 | ||
| US10669289B2 (en) | 2014-10-01 | 2020-06-02 | Merck Patent Gmbh | Boronic acid derivatives |
| US9453018B2 (en) | 2014-10-01 | 2016-09-27 | Bristol-Myers Squibb Company | Pyrimidinones as factor XIa inhibitors |
| JOP20160086B1 (ar) | 2015-05-08 | 2021-08-17 | 2 Katholieke Univ Leuven Ku Leuven Research And Development | مشتقات اندول مستبدلة احاديا او ثنائيا بصفتها مانعات للتكاثر الفيروسي لحمى الفنك |
| WO2016205482A1 (en) | 2015-06-19 | 2016-12-22 | Bristol-Myers Squibb Company | Diamide macrocycles as factor xia inhibitors |
| JP6629958B2 (ja) * | 2015-07-29 | 2020-01-15 | ブリストル−マイヤーズ スクイブ カンパニーＢｒｉｓｔｏｌ−Ｍｙｅｒｓ Ｓｑｕｉｂｂ Ｃｏｍｐａｎｙ | アルキルまたはシクロアルキルＰ２’基を担持する大員環の第ＸＩａ因子阻害剤 |
| CN114874222B (zh) | 2015-07-29 | 2025-06-06 | 百时美施贵宝公司 | 携带非芳族p2,基团的因子xia新大环 |
| JO3633B1 (ar) | 2015-09-16 | 2020-08-27 | Katholieke Univ Leuven Ku Leuven Research & Development | مشتقات اندول مستبدلة احاديا او ثنائيا بصفتها مانعات للتكاثر الفيروسي لحمى الفنك |
| JOP20160198B1 (ar) | 2015-09-16 | 2022-03-14 | Janssen Pharmaceuticals Inc | مشتقات اندول مستبدلة احاديا او ثنائيا بصفتها مانعات للتكاثر الفيروسي لحمى الفنك |
| JP2019507167A (ja) | 2016-03-02 | 2019-03-14 | ブリストル−マイヤーズ スクイブ カンパニーＢｒｉｓｔｏｌ−Ｍｙｅｒｓ Ｓｑｕｉｂｂ Ｃｏｍｐａｎｙ | 第ｘｉａ因子阻害活性を有するジアミド大員環 |
| MA44498A (fr) | 2016-03-31 | 2019-02-06 | Janssen Pharmaceuticals Inc | Dérivés d'indoline substituée utilisés en tant qu'inhibiteurs de la réplication du virus de la dengue |
| EP3436435B1 (en) | 2016-03-31 | 2021-05-12 | Janssen Pharmaceuticals, Inc. | Substituted indole derivatives as dengue viral replication inhibitors |
| SG11201808237UA (en) | 2016-04-01 | 2018-10-30 | Janssen Pharmaceuticals Inc | Substituted indole compound derivatives as dengue viral replication inhibitors |
| JOP20170069B1 (ar) | 2016-04-01 | 2021-08-17 | 1 Janssen Pharmaceuticals Inc | مشتقات اندولين مستبدلة بصفتها مانعات للتكاثر الفيروسي لحمى الفنك |
| WO2018133793A1 (zh) * | 2017-01-18 | 2018-07-26 | 广东东阳光药业有限公司 | 凝血因子XIa抑制剂及其用途 |
| JOP20180026A1 (ar) | 2017-03-31 | 2019-01-30 | Univ Leuven Kath | مشتقات اندولين مستبدلة بصفتها مانعات للتكاثر الفيروسي لحمى الفنك |
| JOP20180025B1 (ar) | 2017-03-31 | 2021-08-17 | Janssen Pharmaceuticals Inc | مشتقات اندولين مستبدلة بصفتها مانعات للتكاثر الفيروسي لحمى الفنك |
| PE20200604A1 (es) | 2017-05-22 | 2020-03-10 | Janssen Pharmaceuticals Inc | Derivados de indolina sustituidos como inhibidores de la replicacion virica de dengue |
| TWI771420B (zh) | 2017-05-22 | 2022-07-21 | 美商健生醫藥公司 | 作為登革熱病毒複製抑制劑之經取代之吲哚啉衍生物（一） |
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| TW201319068A (zh) | 2011-08-05 | 2013-05-16 | 必治妥美雅史谷比公司 | 作為ｘｉａ因子抑制劑之環狀ｐ１接合劑 |
| AU2012356374B2 (en) * | 2011-12-21 | 2017-06-22 | Ono Pharmaceutical Co., Ltd. | Pyridinone and pyrimidinone derivatives as factor XIa inhibitors |
| PL2880026T3 (pl) * | 2012-08-03 | 2017-08-31 | Bristol-Myers Squibb Company | Dihydropirydon P1 jako inhibitory czynnika XIA |
| SG11201500270RA (en) * | 2012-08-03 | 2015-03-30 | Bristol Myers Squibb Co | Dihydropyridone p1 as factor xia inhibitors |
| BR112016015717B1 (pt) * | 2014-01-31 | 2023-04-04 | Bristol-Myers Squibb Company | Compostos macrociclos com grupos p2' heterocíclicos como inibidores do fator xia, composição farmacêutica compreendendo os referidos compostos e uso dos mesmos |
| NO2760821T3 (es) * | 2014-01-31 | 2018-03-10 | ||
| NO2721243T3 (es) * | 2014-10-01 | 2018-10-20 |
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