HRP20192125T1 - URETANI, UREE, AMIDINI I POVEZANI INHIBITORI FAKTORA Xa - Google Patents
URETANI, UREE, AMIDINI I POVEZANI INHIBITORI FAKTORA Xa Download PDFInfo
- Publication number
- HRP20192125T1 HRP20192125T1 HRP20192125TT HRP20192125T HRP20192125T1 HR P20192125 T1 HRP20192125 T1 HR P20192125T1 HR P20192125T T HRP20192125T T HR P20192125TT HR P20192125 T HRP20192125 T HR P20192125T HR P20192125 T1 HRP20192125 T1 HR P20192125T1
- Authority
- HR
- Croatia
- Prior art keywords
- compound
- following structure
- thrombotic
- ome
- hydroxyl
- Prior art date
Links
- 108010074860 Factor Xa Proteins 0.000 title claims 3
- 150000001409 amidines Chemical class 0.000 title 1
- 235000013877 carbamide Nutrition 0.000 title 1
- 239000003112 inhibitor Substances 0.000 title 1
- 150000003672 ureas Chemical class 0.000 title 1
- 150000003673 urethanes Chemical class 0.000 title 1
- 150000001875 compounds Chemical class 0.000 claims 18
- 208000007536 Thrombosis Diseases 0.000 claims 5
- 125000000956 methoxy group Chemical group [H]C([H])([H])O* 0.000 claims 4
- 125000002843 carboxylic acid group Chemical group 0.000 claims 3
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 3
- 241000124008 Mammalia Species 0.000 claims 2
- 206010047249 Venous thrombosis Diseases 0.000 claims 2
- 239000003146 anticoagulant agent Substances 0.000 claims 2
- 230000002401 inhibitory effect Effects 0.000 claims 2
- 239000008194 pharmaceutical composition Substances 0.000 claims 2
- 230000002265 prevention Effects 0.000 claims 2
- 230000002537 thrombolytic effect Effects 0.000 claims 2
- 230000001732 thrombotic effect Effects 0.000 claims 2
- 208000004476 Acute Coronary Syndrome Diseases 0.000 claims 1
- 206010002383 Angina Pectoris Diseases 0.000 claims 1
- 206010002388 Angina unstable Diseases 0.000 claims 1
- 206010053567 Coagulopathies Diseases 0.000 claims 1
- 206010051055 Deep vein thrombosis Diseases 0.000 claims 1
- 206010014498 Embolic stroke Diseases 0.000 claims 1
- 206010062506 Heparin-induced thrombocytopenia Diseases 0.000 claims 1
- 208000010378 Pulmonary Embolism Diseases 0.000 claims 1
- 206010043647 Thrombotic Stroke Diseases 0.000 claims 1
- 201000007023 Thrombotic Thrombocytopenic Purpura Diseases 0.000 claims 1
- 208000032109 Transient ischaemic attack Diseases 0.000 claims 1
- 208000007814 Unstable Angina Diseases 0.000 claims 1
- 239000008280 blood Substances 0.000 claims 1
- 210000004369 blood Anatomy 0.000 claims 1
- 230000023555 blood coagulation Effects 0.000 claims 1
- 208000015294 blood coagulation disease Diseases 0.000 claims 1
- 238000007887 coronary angioplasty Methods 0.000 claims 1
- 208000009190 disseminated intravascular coagulation Diseases 0.000 claims 1
- 238000000338 in vitro Methods 0.000 claims 1
- 201000004332 intermediate coronary syndrome Diseases 0.000 claims 1
- 230000001404 mediated effect Effects 0.000 claims 1
- 238000000034 method Methods 0.000 claims 1
- 208000010125 myocardial infarction Diseases 0.000 claims 1
- 150000003839 salts Chemical class 0.000 claims 1
- 239000012453 solvate Substances 0.000 claims 1
- 208000011580 syndromic disease Diseases 0.000 claims 1
- 238000002560 therapeutic procedure Methods 0.000 claims 1
- 201000010875 transient cerebral ischemia Diseases 0.000 claims 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)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Cardiology (AREA)
- Hematology (AREA)
- Diabetes (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)
Claims (18)
1. Spoj formule I
naznačen time da:
R1 je odabran od H, -Cl, -F, -Br, -OH, -Me, -OMe;
R2 je odabran od CH i N;
R3 i R4 su svaki zasebno odabrani od H, -Cl, -F, -Br, -OH, -Me, -OMe;
R5 je odabran od H ili C1-C6 alkila koji je opcionalno zamjenjiv s hidroksilom, ili skupinom karboksilne kiseline;
R6 od:
X1, X2, X3 i X4 su svaki zasebno H ili C1-C6 alkil koji je opcionalno zamjenjiv s hidroksil-, ili skupinom karboksilne kiseline;
R8, R9 i R10 su svaki zasebno odabrani od H, -Cl, -F, -Br, -OH, -Me, -OMe;
R7 je odabran iz skupine H, -Cl, -F, -Br, -OH, -Me, -OMe ili od:
gdje su Z1, Z2, Z3, Z4, Z5, Z6, Z7, Z8, Z9 i Z10 svaki zasebno H ili C1-C6 alkil koji je opcionalno zamijenjen s hidroksil, ili skupinom karboksilne kiseline; ili spojem koji ima sljedeću strukturu:
i farmaceutski prihvatljivom soli, hidratom, i solvatima istog.
2. Spoj iz zahtjeva 1, koji ima sljedeću strukturu:
3. Spoj iz zahtjeva 1, koji ima sljedeću strukturu:
4. Spoj iz zahtjeva 1, koji ima sljedeću strukturu:
5. Spoj iz zahtjeva 1, koji ima sljedeću strukturu:
6. Spoj iz zahtjeva 1, koji ima sljedeću strukturu:
7. Spoj iz zahtjeva 1, koji ima sljedeću strukturu:
8. Spoj iz zahtjeva 1, koji ima sljedeću strukturu:
9. Spoj iz zahtjeva 1, koji ima sljedeću strukturu:
10. Spoj iz zahtjeva 1, koji ima sljedeću strukturu:
11. Spoj iz zahtjeva 1, koji ima sljedeću strukturu:
12. Spoj iz zahtjeva 1, koji ima sljedeću strukturu:
13. Spoj iz zahtjeva 1, koji ima sljedeću strukturu:
14. Spoj iz zahtjeva 1, koji ima sljedeću strukturu:
15. Farmaceutski sastav za korištenje u prevenciji ili liječenju stanja kod sisavaca naznačenog neželjenom trombozom, obuhvaćajući terapeutski učinkovitu količinu spoja iz bilo kojeg od zahtjeva 1 – 14.
16. Korištenje terapeutski učinkovite količine spoja iz jednog od zahtjeva 1 – 14 u pripremi farmaceutskog sastava za prevenciju ili liječenje stanja kod ljudi i drugih sisavaca naznačenog neželjenom trombozom, s participacijom faktora Xa.
17. Korištenje prema zahtjevu 16, pri čemu je stanje odabrano iz skupine koja obuhvaća: akutni koronarni sindrom, infarkt miokarda, nestabilnu anginu, refraktornu anginu, okluzivan koronarni tromb koji se pojavljuje nakon trombolitičke terapije ili nakon koronarne angioplastike, trombolitički posredovan cerebrovaskularni sindrom, embolijski moždani udar, trombotski moždani udar, tranzitorne ishemičke napade, vensku trombozu, duboku vensku trombozu, plućnu emboliju, koagulopatiju, diseminiranu intravaskularnu koagulaciju, trombotičnu trombocitopeničnu purpuru, obliteracijski trombangitis, trombotične bolesti povezane s trombocitopenijom izazvanom heparinom, trombotične komplikacije povezane s izvantjelesnom cirkulacijom, trombotične komplikacije povezane s postavljanjem protetičkih naprava.
18. Postupak inhibicije zgrušnjavanja krvi in vitro putem inhibicije faktora Xa, obuhvaćajući korak dodavanja krvi spoja iz bilo kojeg od zahtjeva 1 – 14.
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EA201000506A EA015918B1 (ru) | 2010-03-03 | 2010-03-03 | УРЕТАНЫ, МОЧЕВИНЫ, АМИДЫ И РОДСТВЕННЫЕ ИНГИБИТОРЫ ФАКТОРА Xa |
| EP11750982.8A EP2542529B1 (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 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| HRP20192125T1 true HRP20192125T1 (hr) | 2020-02-21 |
Family
ID=44542428
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| HRP20192125TT HRP20192125T1 (hr) | 2010-03-03 | 2019-11-26 | URETANI, UREE, AMIDINI I POVEZANI INHIBITORI FAKTORA Xa |
Country Status (24)
| Country | Link |
|---|---|
| US (1) | US9708265B2 (hr) |
| EP (1) | EP2542529B1 (hr) |
| JP (1) | JP6078707B2 (hr) |
| KR (1) | KR101771760B1 (hr) |
| CN (1) | CN102971294B (hr) |
| AU (1) | AU2011221601B2 (hr) |
| BR (1) | BR112012021884B8 (hr) |
| CA (1) | CA2791875C (hr) |
| CY (1) | CY1122645T1 (hr) |
| DK (1) | DK2542529T3 (hr) |
| EA (1) | EA015918B1 (hr) |
| HK (1) | HK1182700A1 (hr) |
| HR (1) | HRP20192125T1 (hr) |
| HU (1) | HUE047249T2 (hr) |
| IL (1) | IL221727A (hr) |
| LT (1) | LT2542529T (hr) |
| MX (1) | MX2012009976A (hr) |
| NZ (1) | NZ602769A (hr) |
| PL (1) | PL2542529T3 (hr) |
| PT (1) | PT2542529T (hr) |
| SI (1) | SI2542529T1 (hr) |
| UA (1) | UA107106C2 (hr) |
| WO (1) | WO2011108963A1 (hr) |
| ZA (1) | ZA201207345B (hr) |
Families Citing this family (5)
| 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 |
| EA030138B1 (ru) * | 2016-06-15 | 2018-06-29 | Общество С Ограниченной Ответственностью "Фармадиол" | Фармацевтические композиции, включающие антикоагулянт n-(5-хлорпиридин-2-ил)-2-({4-[этанимидоил(метил)амино]бензоил}амино)-5-метилбензамид |
| 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 |
| US5869501A (en) | 1994-12-02 | 1999-02-09 | Yamanouchi Pharmaceutical Co. Ltd | Amidinonaphthyl derivative or salt thereof |
| US5849759A (en) | 1995-12-08 | 1998-12-15 | Berlex Laboratories, Inc. | Naphthyl-substituted benzimidazole derivatives as anti-coagulants |
| CA2275796A1 (en) | 1996-12-23 | 1998-07-02 | Donald Joseph Phillip Pinto | Nitrogen containing heteroaromatics as factor xa inhibitors |
| KR20010023364A (ko) | 1997-08-27 | 2001-03-26 | 간자와 무츠와 | 3-아미디노아닐린 유도체, 활성화 혈액응고 제 ｘ 인자저해제 및 그것의 제조중간체 |
| WO2001019788A2 (en) | 1999-09-17 | 2001-03-22 | Cor Therapeutics, Inc. | BENZAMIDES AND RELATED INHIBITORS OF FACTOR Xa |
| US20020052343A1 (en) * | 1999-12-15 | 2002-05-02 | Allen Darin Arthur | Salicylamides as serine protease inhibitors |
| DE19962924A1 (de) | 1999-12-24 | 2001-07-05 | Bayer Ag | Substituierte Oxazolidinone und ihre Verwendung |
| ES2254385T3 (es) | 2000-02-29 | 2006-06-16 | Millennium Pharmaceuticals, Inc. | Benzamidas e inhibidores relacionados del 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 |
| AU2002350217A1 (en) * | 2001-12-04 | 2003-06-17 | Bristol-Myers Squibb Company | Glycinamides as factor xa inhibitors |
| JPWO2006070878A1 (ja) * | 2004-12-28 | 2008-06-12 | アステラス製薬株式会社 | 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 |
| ATE549317T1 (de) * | 2005-11-08 | 2012-03-15 | Millennium Pharm Inc | Pharmazeutische salze und polymorphe aus n-(5- chloro-2-pyridinyl)-2-ää4- ä(dimethylamino)iminomethylübenzoylüaminoü-5- methoxy-benzamid, einem faktor-xa-hemmer |
| RU2452484C2 (ru) * | 2006-12-08 | 2012-06-10 | Милленниум Фармасьютикалз, Инк. | Стандартные лекарственные препараты и способы лечения тромбоза пероральным введением ингибитора фактора ха |
-
2010
- 2010-03-03 EA EA201000506A patent/EA015918B1/ru unknown
-
2011
- 2011-02-03 UA UAA201211358A patent/UA107106C2/ru unknown
- 2011-03-02 BR BR112012021884A patent/BR112012021884B8/pt active IP Right Grant
- 2011-03-02 SI SI201131816T patent/SI2542529T1/sl unknown
- 2011-03-02 MX MX2012009976A patent/MX2012009976A/es active IP Right Grant
- 2011-03-02 PT PT117509828T patent/PT2542529T/pt unknown
- 2011-03-02 EP EP11750982.8A patent/EP2542529B1/en active Active
- 2011-03-02 LT LT11750982T patent/LT2542529T/lt unknown
- 2011-03-02 AU AU2011221601A patent/AU2011221601B2/en active Active
- 2011-03-02 NZ NZ602769A patent/NZ602769A/en unknown
- 2011-03-02 DK DK11750982.8T patent/DK2542529T3/da active
- 2011-03-02 CN CN201180011928.4A patent/CN102971294B/zh active Active
- 2011-03-02 HU HUE11750982A patent/HUE047249T2/hu unknown
- 2011-03-02 CA CA2791875A patent/CA2791875C/en active Active
- 2011-03-02 JP JP2012556036A patent/JP6078707B2/ja active Active
- 2011-03-02 PL PL11750982T patent/PL2542529T3/pl unknown
- 2011-03-02 KR KR1020127025881A patent/KR101771760B1/ko active IP Right Grant
- 2011-03-02 WO PCT/RU2011/000129 patent/WO2011108963A1/en active Application Filing
-
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
-
2013
- 2013-08-26 HK HK13109973.7A patent/HK1182700A1/xx unknown
-
2019
- 2019-10-03 CY CY20191101032T patent/CY1122645T1/el unknown
- 2019-11-26 HR HRP20192125TT patent/HRP20192125T1/hr unknown
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