ES2655669T3 - Derivados de piridinona y pirimidinona como inhibidores del factor XIa - Google Patents
Derivados de piridinona y pirimidinona como inhibidores del factor XIa Download PDFInfo
- Publication number
- ES2655669T3 ES2655669T3 ES12813423.6T ES12813423T ES2655669T3 ES 2655669 T3 ES2655669 T3 ES 2655669T3 ES 12813423 T ES12813423 T ES 12813423T ES 2655669 T3 ES2655669 T3 ES 2655669T3
- Authority
- ES
- Spain
- Prior art keywords
- alkyl
- alkylene
- nhc
- halogen
- aryl
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Active
Links
- 108010080805 Factor XIa Proteins 0.000 title description 6
- 239000003112 inhibitor Substances 0.000 title 1
- 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
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 abstract description 25
- 229910052736 halogen Inorganic materials 0.000 abstract description 20
- 150000002367 halogens Chemical class 0.000 abstract description 20
- 125000002947 alkylene group Chemical group 0.000 abstract description 17
- 125000000592 heterocycloalkyl group Chemical group 0.000 abstract description 17
- 125000000217 alkyl group Chemical group 0.000 abstract description 16
- 229910052739 hydrogen Inorganic materials 0.000 abstract description 16
- 239000001257 hydrogen Substances 0.000 abstract description 16
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 abstract description 15
- 125000004209 (C1-C8) alkyl group Chemical group 0.000 abstract description 13
- 125000000172 C5-C10 aryl group Chemical group 0.000 abstract description 11
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 abstract description 11
- 150000001875 compounds Chemical class 0.000 abstract description 11
- 125000001313 C5-C10 heteroaryl group Chemical group 0.000 abstract description 10
- 125000006552 (C3-C8) cycloalkyl group Chemical group 0.000 abstract description 9
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 abstract description 7
- 125000004093 cyano group Chemical group *C#N 0.000 abstract description 6
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 abstract description 4
- 150000002431 hydrogen Chemical class 0.000 abstract description 4
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 abstract description 3
- 125000004450 alkenylene group Chemical group 0.000 abstract description 2
- 125000004648 C2-C8 alkenyl group Chemical group 0.000 abstract 7
- 125000004649 C2-C8 alkynyl group Chemical group 0.000 abstract 5
- 125000000753 cycloalkyl group Chemical group 0.000 abstract 3
- 125000000304 alkynyl group Chemical group 0.000 abstract 2
- 150000001204 N-oxides Chemical class 0.000 abstract 1
- 125000003118 aryl group Chemical group 0.000 abstract 1
- -1 cyano, oxo, amidino Chemical group 0.000 abstract 1
- 125000001072 heteroaryl group Chemical group 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 239000012453 solvate Substances 0.000 abstract 1
- 230000000052 comparative effect Effects 0.000 description 4
- ZAMOUSCENKQFHK-UHFFFAOYSA-N Chlorine atom Chemical compound [Cl] ZAMOUSCENKQFHK-UHFFFAOYSA-N 0.000 description 3
- 229910052801 chlorine Inorganic materials 0.000 description 3
- 239000000460 chlorine Substances 0.000 description 3
- 230000002401 inhibitory effect Effects 0.000 description 3
- YNAVUWVOSKDBBP-UHFFFAOYSA-N Morpholine Chemical compound C1COCCN1 YNAVUWVOSKDBBP-UHFFFAOYSA-N 0.000 description 2
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 description 2
- 238000000338 in vitro Methods 0.000 description 2
- PQNFLJBBNBOBRQ-UHFFFAOYSA-N indane Chemical compound C1=CC=C2CCCC2=C1 PQNFLJBBNBOBRQ-UHFFFAOYSA-N 0.000 description 2
- WKBOTKDWSSQWDR-UHFFFAOYSA-N Bromine atom Chemical compound [Br] WKBOTKDWSSQWDR-UHFFFAOYSA-N 0.000 description 1
- PXGOKWXKJXAPGV-UHFFFAOYSA-N Fluorine Chemical compound FF PXGOKWXKJXAPGV-UHFFFAOYSA-N 0.000 description 1
- 238000003556 assay Methods 0.000 description 1
- GDTBXPJZTBHREO-UHFFFAOYSA-N bromine Substances BrBr GDTBXPJZTBHREO-UHFFFAOYSA-N 0.000 description 1
- 229910052794 bromium Inorganic materials 0.000 description 1
- 229910052731 fluorine Inorganic materials 0.000 description 1
- 239000011737 fluorine Substances 0.000 description 1
- 125000004435 hydrogen atom Chemical group [H]* 0.000 description 1
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 description 1
- 230000036470 plasma concentration Effects 0.000 description 1
Classifications
-
- 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
-
- 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
- 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)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Heart & Thoracic Surgery (AREA)
- Cardiology (AREA)
- Epidemiology (AREA)
- Vascular Medicine (AREA)
- Urology & Nephrology (AREA)
- Diabetes (AREA)
- Hematology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
Applications Claiming Priority (5)
| 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 |
| GB201122139 | 2011-12-21 | ||
| GB201217290 | 2012-09-27 | ||
| 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 (1)
| Publication Number | Publication Date |
|---|---|
| ES2655669T3 true ES2655669T3 (es) | 2018-02-21 |
Family
ID=47553259
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ES12813423.6T Active ES2655669T3 (es) | 2011-12-21 | 2012-12-20 | Derivados de piridinona y pirimidinona como inhibidores del factor XIa |
| ES17193874T Active ES2765891T3 (es) | 2011-12-21 | 2012-12-20 | Derivados de piridinona y pirimidinona como inhibidores del factor XIa |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ES17193874T Active ES2765891T3 (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 (2) |
| EP (2) | EP2794597B1 (2) |
| JP (2) | JP6137193B2 (2) |
| KR (1) | KR102011534B1 (2) |
| CN (1) | CN104136431B (2) |
| AU (1) | AU2012356374B2 (2) |
| BR (1) | BR112014015669B1 (2) |
| CA (1) | CA2859604C (2) |
| DK (1) | DK2794597T3 (2) |
| ES (2) | ES2655669T3 (2) |
| HU (1) | HUE036010T2 (2) |
| IL (1) | IL233154A (2) |
| IN (1) | IN2014CN04676A (2) |
| MX (1) | MX351471B (2) |
| NO (1) | NO2794597T3 (2) |
| PH (1) | PH12014501365B1 (2) |
| PL (1) | PL2794597T3 (2) |
| PT (1) | PT2794597T (2) |
| RU (1) | RU2630677C2 (2) |
| SG (1) | SG11201403402VA (2) |
| TW (1) | TWI613199B (2) |
| WO (1) | WO2013093484A1 (2) |
Families Citing this family (70)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| MX2012008874A (es) | 2010-02-11 | 2012-08-31 | Bristol Myers Squibb Co | Macrociclos como inhibidores del factor de coagulacion (fxia). |
| US9062061B2 (en) * | 2011-07-13 | 2015-06-23 | Santen Pharmaceutical Co., Ltd. | Compound having PARP inhibitory activity |
| US9079929B2 (en) | 2011-10-14 | 2015-07-14 | Bristol-Myers Squibb Company | Substituted tetrahydroisoquinoline compounds as factor XIa inhibitors |
| EA023649B1 (ru) | 2011-10-14 | 2016-06-30 | Бристол-Майерс Сквибб Кампани | ЗАМЕЩЕННЫЕ СОЕДИНЕНИЯ ТЕТРАГИДРОИЗОХИНОЛИНА В КАЧЕСТВЕ ИНГИБИТОРОВ ФАКТОРА XIa |
| ES2699226T3 (es) | 2011-10-14 | 2019-02-08 | Bristol Myers Squibb Co | Compuestos de tetrahidroisoquinolina sustituidos como inhibidores del factor XIa |
| WO2013093484A1 (en) * | 2011-12-21 | 2013-06-27 | Ono Pharmaceutical Co., Ltd. | Pyridinone and pyrimidinone derivatives as factor xia inhibitors |
| JP2015503505A (ja) * | 2011-12-23 | 2015-02-02 | ミレニアム ファーマシューティカルズ， インコーポレイテッドＭｉｌｌｅｎｎｉｕｍ Ｐｈａｒｍａｃｅｕｔｉｃａｌｓ， Ｉｎｃ． | ヘテロアリールおよびその使用 |
| CA2881566A1 (en) | 2012-07-19 | 2014-01-23 | Yohei Ikuma | 1-(cycloalkyl-carbonyl)proline derivative |
| EA028581B1 (ru) | 2012-08-03 | 2017-12-29 | Бристол-Маерс Сквибб Компани | ДИГИДРОПИРИДОН Р1 В КАЧЕСТВЕ ИНГИБИТОРОВ ФАКТОРА XIa |
| ES2605824T3 (es) | 2012-08-03 | 2017-03-16 | Bristol-Myers Squibb Company | Dihidropiridona como inhibidores del factor XIa |
| NZ707990A (en) | 2012-10-12 | 2018-07-27 | Bristol Myers Squibb Co | Crystalline forms of a factor xia inhibitor |
| US9315519B2 (en) | 2012-10-12 | 2016-04-19 | Bristol-Myers Squibb Company | Guanidine substituted tetrahydroisoquinoline compounds 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 |
| ES2712699T3 (es) | 2013-03-25 | 2019-05-14 | Bristol Myers Squibb Co | Tetrahidroisoquinolinas que contienen azoles sustituidos como inhibidores del factor XIa |
| EP2978425B1 (en) * | 2013-03-27 | 2017-09-27 | 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 |
| ES2659045T3 (es) * | 2013-10-30 | 2018-03-13 | Bayer Pharma Aktiengesellschaft | Derivados de oxopiridina sustituidos |
| NO2760821T3 (2) | 2014-01-31 | 2018-03-10 | ||
| PE20210470A1 (es) * | 2014-01-31 | 2021-03-08 | Bristol Myers Squibb Co | Macrociclos con grupos p2' heterociclicos como inhibidores del factor xia |
| EP3104702B1 (en) | 2014-02-11 | 2022-08-10 | Merck Sharp & Dohme LLC | Factor xia inhibitors |
| EP3104703B1 (en) | 2014-02-11 | 2020-11-18 | Merck Sharp & Dohme Corp. | Factor xia inhibitors |
| EP3138839B1 (en) * | 2014-02-14 | 2020-10-28 | Sichuan Haisco Pharmaceutical Co., Ltd. | Pyridone or pyrimidone derivative, preparation method therefor and application thereof |
| WO2015164308A1 (en) | 2014-04-22 | 2015-10-29 | Merck Sharp & Dohme Corp. | FACTOR XIa INHIBITORS |
| WO2016011940A1 (zh) * | 2014-07-25 | 2016-01-28 | 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 |
| CN107074821B (zh) | 2014-09-04 | 2020-05-22 | 百时美施贵宝公司 | 为fxia抑制剂的二酰胺大环化合物 |
| 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 |
| ES2713624T3 (es) * | 2014-09-24 | 2019-05-23 | Bayer Pharma AG | Derivados de oxopiridina sustituidos |
| WO2016046158A1 (de) * | 2014-09-24 | 2016-03-31 | Bayer Pharma Aktiengesellschaft | Substituierte oxopyridin-derivate |
| US9453018B2 (en) | 2014-10-01 | 2016-09-27 | Bristol-Myers Squibb Company | Pyrimidinones as factor XIa inhibitors |
| NO2721243T3 (2) * | 2014-10-01 | 2018-10-20 | ||
| CA2970233C (en) * | 2014-12-10 | 2023-01-03 | Ono Pharmaceutical Co., Ltd. | Dihydroindolizinone derivative |
| GB201506660D0 (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 |
| GB201506658D0 (en) | 2015-04-20 | 2015-06-03 | Cellcentric Ltd | Pharmaceutical compounds |
| JO3703B1 (ar) | 2015-07-09 | 2021-01-31 | Bayer Pharma AG | مشتقات أوكسوبيريدين مستبدلة |
| 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 |
| EP3331872B1 (en) | 2015-08-05 | 2019-09-25 | Bristol-Myers Squibb Company | Novel substituted glycine derived fxia inhibitors |
| 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 |
| BR112018008506B8 (pt) | 2015-10-29 | 2023-12-05 | Merck Sharp & Dohme | Compostos inibidores do fator xia, composição farmacêutica e usos dos mesmos |
| 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 |
| EP3500556B1 (en) | 2016-08-22 | 2023-08-02 | Merck Sharp & Dohme LLC | Pyridine-1-oxide derivatives and their use as factor xia inhibitors |
| ES2903283T3 (es) * | 2016-08-31 | 2022-03-31 | Jiangsu Hengrui Medicine Co | Derivado de oxipicolinamida, método de preparación y uso farmacéutico del mismo |
| EP3523134A1 (de) | 2016-10-07 | 2019-08-14 | Mitsubishi HiTec Paper Europe GmbH | Wärmeempfindliches aufzeichnungsmaterial |
| EP3305538A1 (de) | 2016-10-07 | 2018-04-11 | Mitsubishi HiTec Paper Europe GmbH | Wärmeempfindliches aufzeichnungsmaterial |
| CN106950319B (zh) * | 2017-04-20 | 2019-08-30 | 西安科技大学 | 一种检测特鲁曲班光学异构体含量的方法 |
| CN109507345B (zh) * | 2017-09-15 | 2022-08-05 | 万特制药(海南)有限公司 | 重酒石酸卡巴拉汀中间体及其杂质的分离测定方法 |
| BR112020016856A2 (pt) | 2018-02-27 | 2020-12-22 | Jiangsu Hengrui Medicine Co., Ltd. | Forma de cristal do derivado de oxopicolinamida e método de preparação da mesma |
| KR20210028232A (ko) | 2018-07-02 | 2021-03-11 | 지앙수 헨그루이 메디슨 컴퍼니 리미티드 | 옥시피리딘 아미드 유도체의 결정 형태 및 이를 위한 제조 방법 |
| TWI825144B (zh) * | 2018-08-10 | 2023-12-11 | 美商思達利醫藥公司 | 第二型轉麩醯胺酸酶(tg2)抑制劑 |
| WO2020094156A1 (zh) * | 2018-11-11 | 2020-05-14 | 上海海雁医药科技有限公司 | 双杂环取代的吡啶-2(1h)-酮衍生物、其制法与医药上的用途 |
| CA3121447A1 (en) * | 2018-11-30 | 2020-06-04 | Ono Pharmaceutical Co., Ltd. | Novel crystal of (3s)-3-[2-(6-amino-2-fluoropyridin-3-yl)-4-fluoro-1h-imidazol-5-yl]-7-[5-chloro-2-(1h-tetrazol-1-yl)phenyl]-2,3-dihydroindolizin-5(1h)-one |
| 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 |
| CN112028877B (zh) * | 2019-06-04 | 2021-11-26 | 江西济民可信集团有限公司 | 烷氧吡啶酮化合物及其制备方法和用途 |
| BR112021026556A2 (pt) * | 2019-06-28 | 2022-02-15 | Jiangxi Jemincare Group Co Ltd | Composto tricíclico, método de preparação para ele e uso dele |
| WO2021057818A1 (zh) | 2019-09-27 | 2021-04-01 | 深圳信立泰药业股份有限公司 | FXIa抑制剂及其制备方法和医药用途 |
| CN112778277B (zh) * | 2019-11-11 | 2024-04-02 | 江西济民可信集团有限公司 | 环酮并吡啶酮联杂芳环化合物及其制备方法和用途 |
| CA3189771A1 (en) * | 2020-07-22 | 2022-01-27 | Janssen Pharmaceutica Nv | Compounds useful as factor xia inhibitors |
| JP2024125436A (ja) * | 2021-07-20 | 2024-09-19 | 小野薬品工業株式会社 | イミダゾール化合物の製造方法 |
| US11958856B2 (en) | 2021-07-22 | 2024-04-16 | Janssen Pharmaceutica Nv | Substituted 1,2,3,8,9,9a-hexahydro-5H-pyrrolo[1,2-a]azepin-5-ones as factor XIa inhibitors |
| US20230097157A1 (en) * | 2021-07-22 | 2023-03-30 | Janssen Pharmaceutica Nv | Bicyclic Pyridin-2-one and pyrimidin-4-one Derivatives Useful As a Factor XIa Inhibitors |
| CN113735770B (zh) * | 2021-09-30 | 2023-06-06 | 四川大学 | 一种铑催化的4-苯基噁二唑酮与碳酸亚乙烯酯合成1-氨基异喹啉骨架的方法 |
| TWI833610B (zh) * | 2022-03-21 | 2024-02-21 | 大陸商上海濟煜醫藥科技有限公司 | 三并環類化合物製備方法及其中間體 |
| GEAP202516632A (en) | 2022-04-22 | 2025-02-25 | Vertex Pharma | Heteroaryl compounds for the treatment of pain |
| CN116283908A (zh) * | 2023-03-10 | 2023-06-23 | 合肥工业大学 | 一种n-芳香甲基吡啶酮类衍生物及其制备方法与应用 |
| KR20260032556A (ko) | 2023-06-30 | 2026-03-09 | 심천 사루브리스 퍼머수티칼스 컴퍼니 리미티드 | 다치환된 거대환식 화합물 및 이의 제조 방법과 용도 |
| 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 |
Family Cites Families (22)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP0042675A1 (en) | 1980-06-20 | 1981-12-30 | Norton Company | Method of mounting a grinding wheel on a spindle |
| WO1983003968A1 (en) | 1982-05-18 | 1983-11-24 | University Of Florida | Brain-specific drug delivery |
| CA1241120A (en) | 1985-10-01 | 1988-08-23 | Sami A. Aly | Alternate mark inversion (ami) receiver |
| 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 |
| CN100486576C (zh) | 2002-02-14 | 2009-05-13 | 法玛西雅公司 | 作为p38map激酶调节剂的取代吡啶酮类 |
| US7790736B2 (en) | 2003-08-13 | 2010-09-07 | Takeda Pharmaceutical Company Limited | Dipeptidyl peptidase inhibitors |
| GB0420722D0 (en) * | 2004-09-17 | 2004-10-20 | Addex Pharmaceuticals Sa | Novel allosteric modulators |
| AU2005293384A1 (en) | 2004-10-15 | 2006-04-20 | Astrazeneca Ab | Quinoxalines as B Raf inhibitors |
| CA2588713A1 (en) | 2004-11-24 | 2006-06-01 | Vertex Pharmaceuticals Incorporated | 3-[2-(3-acylamino-2-oxo-2h-pyridin-1-yl)-acetylamino]-4-oxo-pentanoic acid derivatives and their use as caspase inhibitors |
| 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 |
| AR058379A1 (es) * | 2005-12-14 | 2008-01-30 | Bristol Myers Squibb Co | Derivados de arilpropionamida arilacrilamida arilpropinamida o arilmetilurea como inhibidores del factor xia. proceso de obtencion y composiciones farmaceuticas. |
| CN101341129B (zh) * | 2005-12-14 | 2011-12-14 | 布里斯托尔-迈尔斯斯奎布公司 | 作为因子xia抑制剂的芳基丙酰胺，芳基丙烯酰胺，芳基丙炔酰胺，或芳基甲基脲类似物 |
| US20080207654A1 (en) * | 2006-11-24 | 2008-08-28 | Takeda Pharmaceutical Company Limited | Heteromonocyclic compound and use thereof |
| JP5342450B2 (ja) * | 2006-12-15 | 2013-11-13 | ブリストル−マイヤーズ スクイブ カンパニー | 第ＸＩａ因子インヒビターとしてのアリールプロピオンアミド、アリールアクリルアミド、アリールプロピンアミド、またはアリールメチルウレアアナログ |
| CN101970433A (zh) | 2007-12-11 | 2011-02-09 | 先灵公司 | γ分泌酶调节剂 |
| EP2265601B1 (en) * | 2008-03-13 | 2012-02-01 | Bristol-Myers Squibb Company | Pyridazine derivatives as factor xia inhibitors |
| US8946426B2 (en) | 2009-02-06 | 2015-02-03 | Janssen Pharmaceuticals, Inc. | Substituted bicyclic heterocyclic compounds as gamma secretase modulators |
| EP2625170A1 (en) * | 2010-10-07 | 2013-08-14 | Takeda Pharmaceutical Company Limited | 1,4-oxazepane derivatives |
| WO2013093484A1 (en) * | 2011-12-21 | 2013-06-27 | Ono Pharmaceutical Co., Ltd. | Pyridinone and pyrimidinone derivatives as factor xia inhibitors |
-
2012
- 2012-12-20 WO PCT/GB2012/053217 patent/WO2013093484A1/en not_active Ceased
- 2012-12-20 HU HUE12813423A patent/HUE036010T2/hu unknown
- 2012-12-20 ES ES12813423.6T patent/ES2655669T3/es active Active
- 2012-12-20 CN CN201280070352.3A patent/CN104136431B/zh not_active Expired - Fee Related
- 2012-12-20 DK DK12813423.6T patent/DK2794597T3/en active
- 2012-12-20 SG SG11201403402VA patent/SG11201403402VA/en unknown
- 2012-12-20 AU AU2012356374A patent/AU2012356374B2/en not_active Ceased
- 2012-12-20 PL PL12813423T patent/PL2794597T3/pl unknown
- 2012-12-20 IN IN4676CHN2014 patent/IN2014CN04676A/en unknown
- 2012-12-20 CA CA2859604A patent/CA2859604C/en active Active
- 2012-12-20 MX MX2014007269A patent/MX351471B/es active IP Right Grant
- 2012-12-20 US US14/366,396 patent/US9732085B2/en not_active Expired - Fee Related
- 2012-12-20 KR KR1020147016952A patent/KR102011534B1/ko not_active Expired - Fee Related
- 2012-12-20 RU RU2014129797A patent/RU2630677C2/ru active
- 2012-12-20 ES ES17193874T patent/ES2765891T3/es active Active
- 2012-12-20 BR BR112014015669-7A patent/BR112014015669B1/pt not_active IP Right Cessation
- 2012-12-20 PT PT128134236T patent/PT2794597T/pt unknown
- 2012-12-20 EP EP12813423.6A patent/EP2794597B1/en not_active Not-in-force
- 2012-12-20 EP EP17193874.9A patent/EP3290413B9/en not_active Not-in-force
- 2012-12-20 TW TW101148629A patent/TWI613199B/zh not_active IP Right Cessation
- 2012-12-20 NO NO12813423A patent/NO2794597T3/no unknown
- 2012-12-20 JP JP2014548196A patent/JP6137193B2/ja not_active Expired - Fee Related
-
2014
- 2014-06-16 IL IL233154A patent/IL233154A/en active IP Right Grant
- 2014-06-16 PH PH12014501365A patent/PH12014501365B1/en unknown
-
2017
- 2017-05-01 JP JP2017091408A patent/JP6447660B2/ja not_active Expired - Fee Related
- 2017-07-07 US US15/644,655 patent/US10717738B2/en not_active Expired - Fee Related
Also Published As
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| ES2655669T3 (es) | Derivados de piridinona y pirimidinona como inhibidores del factor XIa | |
| CY1124404T1 (el) | Παραγωγα χολικου οξεος ως αγωνιστες fxr/tgr5 και μεθοδοι χρησης αυτων | |
| UY32793A (es) | Compuestos inhibidores de los virus flaviviridae, composición farmacéutica que los contiene y sus usos | |
| CO2018000344A2 (es) | Derivados de piperidina 1,4-sustituidos | |
| AR094262A1 (es) | Compuestos antivirales para el tratamiento de la hepatitis c | |
| UY34888A (es) | Inhibidores del virus de la hepatitis c | |
| UY33775A (es) | Inhibidores macrocíclicos de virus flaviviridae, composiciones farmacéuticas que los comprenden y sus usos | |
| DOP2015000158A (es) | Inhibidores de prmt5 y sus usos | |
| DOP2017000151A (es) | Derivados de quinazolina utilizados para tratar el vih | |
| CO6561783A2 (es) | Inhibidores del virus flaviviridae | |
| AR086546A1 (es) | Derivados de 7h-purin-8(9h)-ona como inhibidores de jak | |
| ECSP12012104A (es) | Inhibidores de virus flaviviridae | |
| NI201100137A (es) | Derivados de sulfonamida | |
| AR085960A1 (es) | 1,3-oxazinas como inhibidores de la bace1 y/o de la bace2 | |
| CO7400872A2 (es) | Derivados sustituidos de ftalazin-1(2h)-ona | |
| MX2011010415A (es) | Formulaciones farmaceuticas que comprenden derivados de nitrocatecol y metodos para hacer las mismas. | |
| CR20140133A (es) | Compuestos de piridazinona y sus usos como inhibidores de daao | |
| EA201492170A1 (ru) | Новые замещенные в цикле n-пиридиниламиды в качестве ингибиторов киназ | |
| PH12014501283A1 (en) | 4`-azido, 3``-fluoro substituted nucleoside derivatives as inhibitors of hcv rna replication | |
| AR093408A1 (es) | Derivados de oxazolidin-2-ona-pirimidina | |
| AR083903A1 (es) | Derivados de benzooxazol y benzotiazol sulfonamidas, utiles para tratar trastornos del ritmo cardiaco y cancer, composiciones farmaceuticas que los contienen y metodo para prepararlos | |
| MX2017016370A (es) | Derivados de 4-bencil y 4-benzoil piperidina sustituidos. | |
| MX2018002738A (es) | Derivados de piridin-2-ona fusionados triciclicos, y su uso como inhibidores de brd4. | |
| ES2641372T3 (es) | Inhibidores de replicación viral, su proceso de preparación y sus usos terapéuticos | |
| PH12014500312A1 (en) | Imidazole derivatives as antiviral agents |