EA201000506A1 - УРЕТАНЫ, МОЧЕВИНЫ, АМИДЫ И РОДСТВЕННЫЕ ИНГИБИТОРЫ ФАКТОРА Xa - Google Patents
УРЕТАНЫ, МОЧЕВИНЫ, АМИДЫ И РОДСТВЕННЫЕ ИНГИБИТОРЫ ФАКТОРА XaInfo
- Publication number
- EA201000506A1 EA201000506A1 EA201000506A EA201000506A EA201000506A1 EA 201000506 A1 EA201000506 A1 EA 201000506A1 EA 201000506 A EA201000506 A EA 201000506A EA 201000506 A EA201000506 A EA 201000506A EA 201000506 A1 EA201000506 A1 EA 201000506A1
- Authority
- EA
- Eurasian Patent Office
- Prior art keywords
- diseases
- pharmaceutically acceptable
- factor
- urethanes
- amides
- Prior art date
Links
- 108010074860 Factor Xa Proteins 0.000 title 1
- XSQUKJJJFZCRTK-UHFFFAOYSA-N Urea Chemical compound NC(N)=O XSQUKJJJFZCRTK-UHFFFAOYSA-N 0.000 title 1
- 150000001408 amides Chemical class 0.000 title 1
- 239000004202 carbamide Substances 0.000 title 1
- 239000003112 inhibitor Substances 0.000 title 1
- 150000003673 urethanes Chemical class 0.000 title 1
- 150000001875 compounds Chemical class 0.000 abstract 2
- 208000004476 Acute Coronary Syndrome Diseases 0.000 abstract 1
- 206010002383 Angina Pectoris Diseases 0.000 abstract 1
- 206010002388 Angina unstable Diseases 0.000 abstract 1
- 206010014498 Embolic stroke Diseases 0.000 abstract 1
- 229940123583 Factor Xa inhibitor Drugs 0.000 abstract 1
- 241000124008 Mammalia Species 0.000 abstract 1
- 208000007536 Thrombosis Diseases 0.000 abstract 1
- 208000007814 Unstable Angina Diseases 0.000 abstract 1
- 230000001154 acute effect Effects 0.000 abstract 1
- 239000003146 anticoagulant agent Substances 0.000 abstract 1
- 230000023555 blood coagulation Effects 0.000 abstract 1
- 238000007887 coronary angioplasty Methods 0.000 abstract 1
- 201000010099 disease Diseases 0.000 abstract 1
- 230000006806 disease prevention Effects 0.000 abstract 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 abstract 1
- 201000004332 intermediate coronary syndrome Diseases 0.000 abstract 1
- 230000000302 ischemic effect Effects 0.000 abstract 1
- 239000000203 mixture Substances 0.000 abstract 1
- 208000010125 myocardial infarction Diseases 0.000 abstract 1
- 108090000623 proteins and genes Proteins 0.000 abstract 1
- 102000004169 proteins and genes Human genes 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 208000011580 syndromic disease Diseases 0.000 abstract 1
- 238000002560 therapeutic procedure Methods 0.000 abstract 1
- 230000001732 thrombotic effect Effects 0.000 abstract 1
Classifications
-
- 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
- C07D213/72—Nitrogen atoms
- C07D213/75—Amino or imino radicals, acylated by carboxylic or carbonic acids, or by sulfur or nitrogen analogues thereof, e.g. carbamates
-
- 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
- A61K31/16—Amides, e.g. hydroxamic acids
-
- 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
- A61K31/16—Amides, e.g. hydroxamic acids
- A61K31/17—Amides, e.g. hydroxamic acids having the group >N—C(O)—N< or >N—C(S)—N<, e.g. urea, thiourea, carmustine
-
- 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
-
- 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
- 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
-
- 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
- A61P9/10—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
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (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)
- Epidemiology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Hematology (AREA)
- Diabetes (AREA)
- Cardiology (AREA)
- Heart & Thoracic Surgery (AREA)
- Pulmonology (AREA)
- Urology & Nephrology (AREA)
- Vascular Medicine (AREA)
- Pyridine Compounds (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
Abstract
Данное изобретение относится к новому классу соединений, их фармацевтически приемлемым солям и их фармацевтически приемлемым композициям, которые эффективны как селективные ингибиторы фактора Ха как в изолированном состоянии, так и в комплексе с другими белками. Новые соединения, описанные в изобретении, могут использоваться для лечения и профилактики болезней, таких как острый коронарный синдром, инфаркт миокарда, нестабильная стенокардия, рефракторная стенокардия, тромбозы, вызванные посттромболитической терапией или коронарной ангиопластикой, острый ишемический цереброваскулярный синдром, эмболический инсульт, тромботический инсульт и ряда других болезней у человека и млекопитающих, связанных со свертываемостью крови.
Priority Applications (24)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EA201000506A EA015918B1 (ru) | 2010-03-03 | 2010-03-03 | УРЕТАНЫ, МОЧЕВИНЫ, АМИДЫ И РОДСТВЕННЫЕ ИНГИБИТОРЫ ФАКТОРА Xa |
| UAA201211358A UA107106C2 (uk) | 2010-03-03 | 2011-02-03 | УРЕТАНИ, СЕЧОВИНИ, АМІДИ ТА РОДИННІ ІНГІБІТОРИ ФАКТОРА Xа |
| DK11750982.8T DK2542529T3 (da) | 2010-03-03 | 2011-03-02 | Urethaner, urinstoffer, amidiner og relaterede inhibitorer af faktor xa |
| CN201180011928.4A CN102971294B (zh) | 2010-03-03 | 2011-03-02 | 氨基甲酸乙酯、尿素、脒和因子Xa的相关抑制剂 |
| JP2012556036A JP6078707B2 (ja) | 2010-03-03 | 2011-03-02 | 第Xa因子のウレタン、尿素、アミジン、及び関連阻害剤 |
| SI201131816T SI2542529T1 (sl) | 2010-03-03 | 2011-03-02 | Uretani, uree, amidini in sorodni inhibitorji faktorja Xa |
| CA2791875A CA2791875C (en) | 2010-03-03 | 2011-03-02 | Urethanes, ureas, amidines and related inhibitors of factor xa |
| LT11750982T LT2542529T (lt) | 2010-03-03 | 2011-03-02 | Uretanai, karbamidai, amidinai ir faktoriaus xa giminingi inhibitoriai |
| MX2012009976A MX2012009976A (es) | 2010-03-03 | 2011-03-02 | Uretanos, ureas, amidinas e inhibidores relacionados del factor xa. |
| PT117509828T PT2542529T (pt) | 2010-03-03 | 2011-03-02 | Uretanos, ureias, amidinas e inibidores relacionados do fator xa |
| AU2011221601A AU2011221601B2 (en) | 2010-03-03 | 2011-03-02 | Urethanes, ureas, amidines and related inhibitors of factor Xa |
| PCT/RU2011/000129 WO2011108963A1 (en) | 2010-03-03 | 2011-03-02 | Urethanes, ureas, amidines and related inhibitors of factor xa |
| EP11750982.8A EP2542529B1 (en) | 2010-03-03 | 2011-03-02 | Urethanes, ureas, amidines and related inhibitors of factor xa |
| HK13109973.7A HK1182700B (en) | 2010-03-03 | 2011-03-02 | Urethanes, ureas, amidines and related inhibitors of factor xa |
| KR1020127025881A KR101771760B1 (ko) | 2010-03-03 | 2011-03-02 | 우레탄, 요소, 아미딘 및 관련된 Xa 인자의 억제제 |
| BR112012021884A BR112012021884B8 (pt) | 2010-03-03 | 2011-03-02 | Composto, composição farmacêutica e método para afetar a coagulação sanguínea ou coagulação de plasma sanguíneo |
| HUE11750982A HUE047249T2 (hu) | 2010-03-03 | 2011-03-02 | Uretánok, karbamidok, amidinek és rokon Xa faktor inhibitorok |
| PL11750982T PL2542529T3 (pl) | 2010-03-03 | 2011-03-02 | Uretany, moczniki, amidyny i powiązane inhibitory czynnika Xa |
| NZ602769A NZ602769A (en) | 2010-03-03 | 2011-03-02 | Urethanes, ureas, amidines and related inhibitors of factor xa |
| HRP20192125TT HRP20192125T1 (hr) | 2010-03-03 | 2011-03-02 | URETANI, UREE, AMIDINI I POVEZANI INHIBITORI FAKTORA Xa |
| US13/599,038 US9708265B2 (en) | 2010-03-03 | 2012-08-30 | Urethanes, ureas, amidines and related inhibitors of factor Xa |
| IL221727A IL221727A (en) | 2010-03-03 | 2012-08-30 | Compounds of urethane ureas, amidines and related inhibitors of factor xa, pharmaceutical preparations containing the compounds, use and method |
| ZA2012/07345A ZA201207345B (en) | 2010-03-03 | 2012-10-01 | Urethanes,ureas,amidines and related inhibitors of factor xa |
| CY20191101032T CY1122645T1 (el) | 2010-03-03 | 2019-10-03 | Oyρεθανες, ουριες, αμιδινες και σχετικοι αναστολεις του παραγοντα χα |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EA201000506A EA015918B1 (ru) | 2010-03-03 | 2010-03-03 | УРЕТАНЫ, МОЧЕВИНЫ, АМИДЫ И РОДСТВЕННЫЕ ИНГИБИТОРЫ ФАКТОРА Xa |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| EA201000506A1 true EA201000506A1 (ru) | 2011-10-31 |
| EA015918B1 EA015918B1 (ru) | 2011-12-30 |
Family
ID=44542428
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| EA201000506A EA015918B1 (ru) | 2010-03-03 | 2010-03-03 | УРЕТАНЫ, МОЧЕВИНЫ, АМИДЫ И РОДСТВЕННЫЕ ИНГИБИТОРЫ ФАКТОРА Xa |
Country Status (23)
| Country | Link |
|---|---|
| US (1) | US9708265B2 (ru) |
| EP (1) | EP2542529B1 (ru) |
| JP (1) | JP6078707B2 (ru) |
| KR (1) | KR101771760B1 (ru) |
| CN (1) | CN102971294B (ru) |
| AU (1) | AU2011221601B2 (ru) |
| BR (1) | BR112012021884B8 (ru) |
| CA (1) | CA2791875C (ru) |
| CY (1) | CY1122645T1 (ru) |
| DK (1) | DK2542529T3 (ru) |
| EA (1) | EA015918B1 (ru) |
| HR (1) | HRP20192125T1 (ru) |
| HU (1) | HUE047249T2 (ru) |
| IL (1) | IL221727A (ru) |
| LT (1) | LT2542529T (ru) |
| MX (1) | MX2012009976A (ru) |
| NZ (1) | NZ602769A (ru) |
| PL (1) | PL2542529T3 (ru) |
| PT (1) | PT2542529T (ru) |
| SI (1) | SI2542529T1 (ru) |
| UA (1) | UA107106C2 (ru) |
| WO (1) | WO2011108963A1 (ru) |
| ZA (1) | ZA201207345B (ru) |
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2017217895A1 (en) * | 2016-06-15 | 2017-12-21 | "Pharmadiall" Ltd | Pharmaceutical compositions comprising anticoagulant n-(5-chloropyridine-2-yl)-2-({4-[ethanimidoil(methyl)amino]benzoyl}amino)-5-methylbenzamide |
Families Citing this family (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2014003153A1 (ja) * | 2012-06-28 | 2014-01-03 | 協和発酵キリン株式会社 | 置換アミド化合物 |
| RU2698202C2 (ru) * | 2016-06-01 | 2019-08-23 | Закрытое акционерное общество "ФАРМА ВАМ" | СПОСОБ ПОЛУЧЕНИЯ ПРЯМОГО ИНГИБИТОРА ФАКТОРА Ха |
| RU2659161C1 (ru) | 2017-11-17 | 2018-06-28 | Общество С Ограниченной Ответственностью "Ива Фарм" | Фармацевтическая композиция, включающая дисульфид глутатиона и глутатион дисульфид s-оксид |
| EA201800084A1 (ru) * | 2018-01-19 | 2019-07-31 | Общество С Ограниченной Ответственностью "Фармадиол" | НОВЫЕ АМИДИНЫ-ИНГИБИТОРЫ ФАКТОРА Ха |
Family Cites Families (16)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US4588587A (en) | 1983-03-01 | 1986-05-13 | Pennsylvania Hospital | Method of treatment to inhibit metastasis |
| TW300888B (ru) | 1994-12-02 | 1997-03-21 | Yamanouchi Pharma Co Ltd | |
| US5849759A (en) | 1995-12-08 | 1998-12-15 | Berlex Laboratories, Inc. | Naphthyl-substituted benzimidazole derivatives as anti-coagulants |
| KR20000062284A (ko) | 1996-12-23 | 2000-10-25 | 블레어 큐. 퍼거슨 | 인자 Xa 억제제로서의 질소 함유 헤테로방향족 화합물 |
| AU8747598A (en) | 1997-08-27 | 1999-03-16 | Kissei Pharmaceutical Co. Ltd. | 3-amidinoaniline derivatives, activated blood coagulation factor x inhibitors, and intermediates for producing both |
| HU230773B1 (hu) | 1999-09-17 | 2018-03-28 | Millennium Pharmaceuticals, Inc. | Benzamidok és rokon Xa faktor inhibitorok |
| EP1242366A1 (en) * | 1999-12-15 | 2002-09-25 | Axys Pharmaceuticals, Inc. | Salicylamides as serine protease and factor xa inhibitors |
| DE19962924A1 (de) | 1999-12-24 | 2001-07-05 | Bayer Ag | Substituierte Oxazolidinone und ihre Verwendung |
| US6376515B2 (en) | 2000-02-29 | 2002-04-23 | Cor Therapeutics, Inc. | Benzamides and related inhibitors of factor Xa |
| DE10063008A1 (de) * | 2000-12-16 | 2002-06-20 | Merck Patent Gmbh | Carbonsäureamidderivate |
| TWI331526B (en) | 2001-09-21 | 2010-10-11 | Bristol Myers Squibb Pharma Co | Lactam-containing compounds and derivatives thereof as factor xa inhibitors |
| WO2003048081A2 (en) * | 2001-12-04 | 2003-06-12 | Bristol-Myers Squibb Company | Glycinamides as factor xa inhibitors |
| WO2006070878A1 (ja) * | 2004-12-28 | 2006-07-06 | Astellas Pharma Inc. | カルボン酸誘導体またはその塩 |
| DE102005042583A1 (de) * | 2005-09-08 | 2007-03-15 | Bayer Healthcare Ag | Iminooxazolidin-Derivate und ihre Verwendung |
| US7598276B2 (en) * | 2005-11-08 | 2009-10-06 | Millenium Pharmaceuticals, Inc. | Pharmaceutical salts and polymorphs of a factor Xa inhibitor |
| CA2671502C (en) * | 2006-12-08 | 2017-01-24 | Millennium Pharmaceuticals, Inc. | Unit dose formulations and methods of treating thrombosis with an oral factor xa inhibitor |
-
2010
- 2010-03-03 EA EA201000506A patent/EA015918B1/ru unknown
-
2011
- 2011-02-03 UA UAA201211358A patent/UA107106C2/ru unknown
- 2011-03-02 DK DK11750982.8T patent/DK2542529T3/da active
- 2011-03-02 SI SI201131816T patent/SI2542529T1/sl unknown
- 2011-03-02 KR KR1020127025881A patent/KR101771760B1/ko active Active
- 2011-03-02 PT PT117509828T patent/PT2542529T/pt unknown
- 2011-03-02 BR BR112012021884A patent/BR112012021884B8/pt not_active IP Right Cessation
- 2011-03-02 NZ NZ602769A patent/NZ602769A/en unknown
- 2011-03-02 JP JP2012556036A patent/JP6078707B2/ja active Active
- 2011-03-02 PL PL11750982T patent/PL2542529T3/pl unknown
- 2011-03-02 HU HUE11750982A patent/HUE047249T2/hu unknown
- 2011-03-02 MX MX2012009976A patent/MX2012009976A/es active IP Right Grant
- 2011-03-02 CN CN201180011928.4A patent/CN102971294B/zh active Active
- 2011-03-02 CA CA2791875A patent/CA2791875C/en active Active
- 2011-03-02 AU AU2011221601A patent/AU2011221601B2/en active Active
- 2011-03-02 WO PCT/RU2011/000129 patent/WO2011108963A1/en not_active Ceased
- 2011-03-02 LT LT11750982T patent/LT2542529T/lt unknown
- 2011-03-02 HR HRP20192125TT patent/HRP20192125T1/hr unknown
- 2011-03-02 EP EP11750982.8A patent/EP2542529B1/en active Active
-
2012
- 2012-08-30 IL IL221727A patent/IL221727A/en active IP Right Grant
- 2012-08-30 US US13/599,038 patent/US9708265B2/en active Active
- 2012-10-01 ZA ZA2012/07345A patent/ZA201207345B/en unknown
-
2019
- 2019-10-03 CY CY20191101032T patent/CY1122645T1/el unknown
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2017217895A1 (en) * | 2016-06-15 | 2017-12-21 | "Pharmadiall" Ltd | Pharmaceutical compositions comprising anticoagulant n-(5-chloropyridine-2-yl)-2-({4-[ethanimidoil(methyl)amino]benzoyl}amino)-5-methylbenzamide |
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