MX351471B - Derivados de piridinona y pirimidinona como inhibidores del factor xia. - Google Patents
Derivados de piridinona y pirimidinona como inhibidores del factor xia.Info
- Publication number
- MX351471B MX351471B MX2014007269A MX2014007269A MX351471B MX 351471 B MX351471 B MX 351471B MX 2014007269 A MX2014007269 A MX 2014007269A MX 2014007269 A MX2014007269 A MX 2014007269A MX 351471 B MX351471 B MX 351471B
- Authority
- MX
- Mexico
- Prior art keywords
- pyridinone
- factor xia
- xia inhibitors
- pyrimidinone derivatives
- inhibitors
- Prior art date
Links
- 108010080805 Factor XIa Proteins 0.000 title abstract 2
- 239000003112 inhibitor Substances 0.000 title abstract 2
- UBQKCCHYAOITMY-UHFFFAOYSA-N pyridin-2-ol Chemical compound OC1=CC=CC=N1 UBQKCCHYAOITMY-UHFFFAOYSA-N 0.000 title 1
- VTGOHKSTWXHQJK-UHFFFAOYSA-N pyrimidin-2-ol Chemical class OC1=NC=CC=N1 VTGOHKSTWXHQJK-UHFFFAOYSA-N 0.000 title 1
- 150000001875 compounds Chemical class 0.000 abstract 2
- 208000001435 Thromboembolism Diseases 0.000 abstract 1
- 230000002265 prevention Effects 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
- 238000002560 therapeutic procedure Methods 0.000 abstract 1
Classifications
-
- 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
- A61K31/495—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
- 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
-
- 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
-
- 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
- C07D403/14—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 three or more hetero rings
-
- 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
- C07D471/02—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 two hetero rings
- C07D471/04—Ortho-condensed systems
-
- 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
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Cardiology (AREA)
- Heart & Thoracic Surgery (AREA)
- Epidemiology (AREA)
- Vascular Medicine (AREA)
- Urology & Nephrology (AREA)
- Diabetes (AREA)
- Hematology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Plural Heterocyclic Compounds (AREA)
Abstract
La presente invención se refiere a compuestos de la fórmula general (I), sus sales y N-óxidos, y solvatos y profármacos de los mismos (en donde los caracteres son como se definen en la descripción). Los compuestos de la fórmula general (I) son inhibidores del Factor XIa de manera que son útiles en la prevención de y/o terapia para enfermedades tromboembólicas. (ver Fórmula).
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| GB1122139.7A GB2497806A (en) | 2011-12-21 | 2011-12-21 | Pyridinone and pyrimidinone derivatives as factor XIa inhibitors |
| GB201217290A GB201217290D0 (en) | 2012-09-27 | 2012-09-27 | Compounds |
| PCT/GB2012/053217 WO2013093484A1 (en) | 2011-12-21 | 2012-12-20 | Pyridinone and pyrimidinone derivatives as factor xia inhibitors |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| MX2014007269A MX2014007269A (es) | 2014-07-22 |
| MX351471B true MX351471B (es) | 2017-10-17 |
Family
ID=47553259
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| MX2014007269A MX351471B (es) | 2011-12-21 | 2012-12-20 | Derivados de piridinona y pirimidinona como inhibidores del factor xia. |
Country Status (22)
| Country | Link |
|---|---|
| US (2) | US9732085B2 (es) |
| EP (2) | EP2794597B1 (es) |
| JP (2) | JP6137193B2 (es) |
| KR (1) | KR102011534B1 (es) |
| CN (1) | CN104136431B (es) |
| AU (1) | AU2012356374B2 (es) |
| BR (1) | BR112014015669B1 (es) |
| CA (1) | CA2859604C (es) |
| DK (1) | DK2794597T3 (es) |
| ES (2) | ES2765891T3 (es) |
| HU (1) | HUE036010T2 (es) |
| IL (1) | IL233154A (es) |
| IN (1) | IN2014CN04676A (es) |
| MX (1) | MX351471B (es) |
| NO (1) | NO2794597T3 (es) |
| PH (1) | PH12014501365A1 (es) |
| PL (1) | PL2794597T3 (es) |
| PT (1) | PT2794597T (es) |
| RU (1) | RU2630677C2 (es) |
| SG (1) | SG11201403402VA (es) |
| TW (1) | TWI613199B (es) |
| WO (1) | WO2013093484A1 (es) |
Families Citing this family (70)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP2534152B1 (en) | 2010-02-11 | 2018-05-02 | Bristol-Myers Squibb Company | Macrocycles as factor xia inhibitors |
| ES2562903T3 (es) * | 2011-07-13 | 2016-03-09 | Santen Pharmaceutical Co., Ltd | Nuevo compuesto que tiene actividad inhibidora de PARP |
| ES2699226T3 (es) | 2011-10-14 | 2019-02-08 | Bristol Myers Squibb Co | Compuestos de tetrahidroisoquinolina sustituidos como inhibidores del factor XIa |
| IN2014CN02805A (es) | 2011-10-14 | 2015-07-03 | Bristol Myers Squibb Co | |
| CN103974938B (zh) | 2011-10-14 | 2016-11-09 | 百时美施贵宝公司 | 作为因子xia抑制剂的经取代的四氢异喹啉化合物 |
| CN104136431B (zh) * | 2011-12-21 | 2017-03-15 | 小野药品工业株式会社 | 作为凝血因子XIa抑制剂的吡啶酮和嘧啶酮衍生物 |
| WO2013096642A1 (en) * | 2011-12-23 | 2013-06-27 | Millennium Pharmaceuticals, Inc. | Heteroaryls and uses thereof |
| AU2013291098A1 (en) | 2012-07-19 | 2015-02-05 | Sumitomo Dainippon Pharma Co., Ltd. | 1-(cycloalkyl-carbonyl)proline derivative |
| SG11201500270RA (en) | 2012-08-03 | 2015-03-30 | Bristol Myers Squibb Co | Dihydropyridone p1 as factor xia inhibitors |
| US9409908B2 (en) | 2012-08-03 | 2016-08-09 | Bristol-Myers Squibb Company | Dihydropyridone p1 as factor XIa inhibitors |
| WO2014059214A1 (en) | 2012-10-12 | 2014-04-17 | Bristol-Myers Squibb Company | Guanidine and amine substituted tetrahydroisoquinoline compounds as factor xia inhibitors |
| JP6154473B2 (ja) | 2012-10-12 | 2017-06-28 | 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因子阻害剤の結晶形 |
| US9315519B2 (en) | 2012-10-12 | 2016-04-19 | Bristol-Myers Squibb Company | Guanidine substituted tetrahydroisoquinoline compounds as factor XIa inhibitors |
| ES2712699T3 (es) | 2013-03-25 | 2019-05-14 | Bristol Myers Squibb Co | Tetrahidroisoquinolinas que contienen azoles sustituidos como inhibidores del factor XIa |
| WO2014160592A2 (en) | 2013-03-27 | 2014-10-02 | Merck Sharp & Dohme Corp. | FACTOR XIa INHIBITORS |
| TWI633089B (zh) * | 2013-03-28 | 2018-08-21 | 拜耳製藥股份有限公司 | 經取代的酮基吡啶衍生物 |
| US9475809B2 (en) * | 2013-07-23 | 2016-10-25 | Bayer Pharma Aktiengesellschaft | Substituted oxopyridine derivatives and use thereof as factor xia/plasma |
| WO2015063093A1 (de) * | 2013-10-30 | 2015-05-07 | Bayer Pharma Aktiengesellschaft | Substituierte oxopyridin-derivate |
| NO2760821T3 (es) | 2014-01-31 | 2018-03-10 | ||
| TWI688564B (zh) * | 2014-01-31 | 2020-03-21 | 美商必治妥美雅史谷比公司 | 作為凝血因子xia抑制劑之具有雜環p2'基團之巨環化合物 |
| US9676723B2 (en) | 2014-02-11 | 2017-06-13 | Merck Sharp & Dohme Corp | Factor XIa inhibitors |
| US9944643B2 (en) | 2014-02-11 | 2018-04-17 | Merck Sharp & Dohme Corp. | Factor XIa inhibitors |
| CN105829298B (zh) | 2014-02-14 | 2019-02-01 | 四川海思科制药有限公司 | 一种吡啶酮或嘧啶酮衍生物、及其制备方法和应用 |
| EP3134408B1 (en) | 2014-04-22 | 2020-08-12 | Merck Sharp & Dohme Corp. | FACTOR XIa INHIBITORS |
| CN105658641B (zh) * | 2014-07-25 | 2018-04-17 | 江苏恒瑞医药股份有限公司 | 氮茚‑酰胺类衍生物、其制备方法及其在医药上的应用 |
| US9868727B2 (en) | 2014-07-28 | 2018-01-16 | Merck Sharp & Dohme Corp. | Factor XIa inhibitors |
| WO2016036893A1 (en) | 2014-09-04 | 2016-03-10 | Bristol-Myers Squibb Company | Diamide macrocycles that are fxia inhibitors |
| CN104311537B (zh) * | 2014-09-19 | 2016-08-24 | 广东东阳光药业有限公司 | 含有嘧啶酮乙酰基取代基吡唑类化合物及其组合物及用途 |
| EP3197896B1 (de) | 2014-09-24 | 2019-01-30 | Bayer Pharma Aktiengesellschaft | Substituierte oxopyridin-derivate |
| CN106687458B (zh) * | 2014-09-24 | 2020-10-27 | 拜耳制药股份公司 | 取代的氧代吡啶衍生物 |
| US9453018B2 (en) | 2014-10-01 | 2016-09-27 | Bristol-Myers Squibb Company | Pyrimidinones as factor XIa inhibitors |
| NO2721243T3 (es) * | 2014-10-01 | 2018-10-20 | ||
| EP3231803B1 (en) | 2014-12-10 | 2020-07-01 | ONO Pharmaceutical Co., Ltd. | Dihydroindolizinone derivative |
| GB201506660D0 (en) | 2015-04-20 | 2015-06-03 | Cellcentric Ltd | Pharmaceutical compounds |
| GB201506658D0 (en) | 2015-04-20 | 2015-06-03 | Cellcentric Ltd | Pharmaceutical compounds |
| RU2649141C2 (ru) * | 2015-04-20 | 2018-03-30 | государственное бюджетное образовательное учреждение высшего профессионального образования "Пермская государственная фармацевтическая академия" Министерства здравоохранения Российской Федерации (ГБОУ ВПО ПГФА Минздрава России) | 3,4-диметил-6-(3-пиридил)-N-фенил-2-оксо-1,2,3,6-тетрагидропиримидин-5-карбоксамид, проявляющий противогрибковое действие в отношении штамма Candida albicans |
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| RU2653511C2 (ru) * | 2015-07-29 | 2018-05-10 | государственное бюджетное образовательное учреждение высшего профессионального образования "Пермская государственная фармацевтическая академия" Министерства здравоохранения Российской Федерации (ГБОУ ВПО ПГФА Минздрава России) | 4-метил-n-2,4-диметилфенил-6-(3-фторфенил)-2-тиоксо-1,2,3,6-тетрагидропиримидин-5-карбоксамид, проявляющий анальгетическое действие |
| JP6785838B2 (ja) | 2015-08-05 | 2020-11-18 | ブリストル−マイヤーズ スクイブ カンパニーBristol−Myers Squibb Company | 新規な置換グリシン誘導のfxia阻害剤 |
| CN106496249B (zh) * | 2015-09-07 | 2019-12-13 | 江苏恒瑞医药股份有限公司 | 噁唑并吲哚类衍生物、其制备方法及其在医药上的应用 |
| EP3371162B1 (en) * | 2015-10-29 | 2022-01-26 | Merck Sharp & Dohme Corp. | Macrocyclic spirocarbamate derivatives as factor xia inhibitors, pharmaceutically acceptable compositions and their use |
| AU2016344476B2 (en) | 2015-10-29 | 2020-08-13 | Merck Sharp & Dohme Llc | Factor XIa inhibitors |
| JP6992284B2 (ja) * | 2016-06-06 | 2022-01-13 | 小野薬品工業株式会社 | ジヒドロインドリジノン誘導体を含有する医薬組成物 |
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| HUE057289T2 (hu) | 2016-08-31 | 2022-05-28 | Jiangsu Hengrui Medicine Co | Oxopikolinamid-származék, annak elõállítási módszere és gyógyszerészeti felhasználása |
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| EP3305538A1 (de) | 2016-10-07 | 2018-04-11 | Mitsubishi HiTec Paper Europe GmbH | Wärmeempfindliches aufzeichnungsmaterial |
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| TWI826599B (zh) | 2018-11-30 | 2023-12-21 | 日商小野藥品工業股份有限公司 | (3s)-3-[2-(6-胺-2-氟吡啶-3-基)-4-氟-1h-咪唑-5-基]-7-[5-氯-2-(1h-四唑-1-基)苯基]-2,3-二氫吲嗪-5(1h)-酮的新穎結晶 |
| CN109836360B (zh) * | 2019-03-19 | 2021-08-13 | 南京恩泰医药科技有限公司 | 一种甲苯磺酸依度沙班中间体的制备方法及中间体化合物 |
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| CN119894901A (zh) | 2023-06-30 | 2025-04-25 | 深圳信立泰药业股份有限公司 | 一种多取代的大环化合物及其制备方法与应用 |
| CN118406037B (zh) * | 2024-06-25 | 2025-02-25 | 四川师范大学 | 一种三氮唑类衍生物及其制备方法和用途 |
| CN118894814B (zh) * | 2024-07-15 | 2025-09-12 | 上海康鹏科技股份有限公司 | 1-(2-溴-4-氯苯基)-4-(三氟甲基)-1h-1,2,3-三唑的制备方法 |
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| CA1334092C (en) * | 1986-07-11 | 1995-01-24 | David John Carini | Angiotensin ii receptor blocking imidazoles |
| EP0407342A3 (en) * | 1989-07-06 | 1991-07-10 | Ciba-Geigy Ag | Pyrimidine derivatives |
| DE4221583A1 (de) * | 1991-11-12 | 1993-05-13 | Bayer Ag | Substituierte biphenylpyridone |
| DE4407488A1 (de) * | 1994-03-07 | 1995-09-14 | Bayer Ag | Verwendung von Biphenyl- und Pyridylmethylpyridonen |
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| EP1506967B1 (en) | 2003-08-13 | 2007-11-21 | Takeda Pharmaceutical Company Limited | Dipeptidyl peptidase inhibitors |
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| AR056682A1 (es) | 2005-07-29 | 2007-10-17 | Kalypsys Inc | COMPUESTOS MULTICíCLICOS DERIVADOS DE LA SULFONAMIDA COMO INHIBIDORES DE LA HISTONA DESACETILASA Y COMPOSICIoN FARMACÉUTICA |
| ES2365815T3 (es) * | 2005-12-14 | 2011-10-11 | Bristol-Myers Squibb Company | Análogos de arilpropionamida, arilacrilamida, arilpropinamida o arilmetilurea como inhibidores del factor xia. |
| US7626039B2 (en) | 2005-12-14 | 2009-12-01 | Bristol-Myers Squibb Company | Arylpropionamide, arylacrylamide, ayrlpropynamide, or arylmethylurea analogs as factor XIa inhibitors |
| MX2009005449A (es) * | 2006-11-24 | 2009-06-02 | Takeda Pharmaceutical | Compuesto heteromonociclico y uso del mismo. |
| WO2008076805A2 (en) | 2006-12-15 | 2008-06-26 | Bristol-Myers Squibb Company | Arylpropionamide, arylacrylamide, arylpropynamide, or arylmethylurea analogs as factor xia inhibitors |
| CA2708151A1 (en) | 2007-12-11 | 2009-06-18 | Schering Corporation | Gamma secretase modulators |
| WO2009114677A1 (en) * | 2008-03-13 | 2009-09-17 | Bristol-Myers Squibb Company | Pyridazine derivatives as factor xia inhibitors |
| WO2010089292A1 (en) | 2009-02-06 | 2010-08-12 | Ortho-Mcneil-Janssen Pharmaceuticals, Inc | Novel substituted bicyclic heterocyclic compounds as gamma secretase modulators |
| AU2011313150A1 (en) * | 2010-10-07 | 2013-04-18 | Takeda Pharmaceutical Company Limited | 1,4-oxazepane derivatives |
| CN104136431B (zh) * | 2011-12-21 | 2017-03-15 | 小野药品工业株式会社 | 作为凝血因子XIa抑制剂的吡啶酮和嘧啶酮衍生物 |
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