HUP9904066A2 - Naftilcsoporttal szubsztituált benzimidazolszármazékok mint véralvadás-gátlók és alkalmazásuk - Google Patents
Naftilcsoporttal szubsztituált benzimidazolszármazékok mint véralvadás-gátlók és alkalmazásukInfo
- Publication number
- HUP9904066A2 HUP9904066A2 HU9904066A HUP9904066A HUP9904066A2 HU P9904066 A2 HUP9904066 A2 HU P9904066A2 HU 9904066 A HU9904066 A HU 9904066A HU P9904066 A HUP9904066 A HU P9904066A HU P9904066 A2 HUP9904066 A2 HU P9904066A2
- Authority
- HU
- Hungary
- Prior art keywords
- benzimidazole derivatives
- anticoagulants
- naphthyl
- powder
- substituted benzimidazole
- Prior art date
Links
- 229940058303 antinematodal benzimidazole derivative Drugs 0.000 title abstract 2
- 125000003785 benzimidazolyl group Chemical class N1=C(NC2=C1C=CC=C2)* 0.000 title abstract 2
- 239000003146 anticoagulant agent Substances 0.000 title 1
- 229940127219 anticoagulant drug Drugs 0.000 title 1
- 239000000843 powder Substances 0.000 abstract 4
- 125000004435 hydrogen atom Chemical group [H]* 0.000 abstract 2
- 125000000547 substituted alkyl group Chemical group 0.000 abstract 2
- VLRSADZEDXVUPG-UHFFFAOYSA-N 2-naphthalen-1-ylpyridine Chemical group N1=CC=CC=C1C1=CC=CC2=CC=CC=C12 VLRSADZEDXVUPG-UHFFFAOYSA-N 0.000 abstract 1
- RWNISPVLLBWJBU-UHFFFAOYSA-N 2-sulfonyl-1h-pyridine Chemical compound O=S(=O)=C1C=CC=CN1 RWNISPVLLBWJBU-UHFFFAOYSA-N 0.000 abstract 1
- 125000005073 adamantyl group Chemical group C12(CC3CC(CC(C1)C3)C2)* 0.000 abstract 1
- 125000003342 alkenyl group Chemical group 0.000 abstract 1
- 125000002947 alkylene group Chemical group 0.000 abstract 1
- 125000002102 aryl alkyloxo group Chemical group 0.000 abstract 1
- 125000004104 aryloxy group Chemical group 0.000 abstract 1
- 125000002915 carbonyl group Chemical group [*:2]C([*:1])=O 0.000 abstract 1
- 125000000753 cycloalkyl group Chemical group 0.000 abstract 1
- 125000000623 heterocyclic group Chemical group 0.000 abstract 1
- -1 imidazolyl- Chemical group 0.000 abstract 1
- 239000003112 inhibitor Substances 0.000 abstract 1
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
Classifications
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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
- A61K31/435—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
- A61K31/445—Non condensed piperidines, e.g. piperocaine
-
- 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
- C07D401/02—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 two hetero rings
- C07D401/12—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 two hetero rings linked by a chain containing hetero atoms as chain links
-
- 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
-
- 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C257/00—Compounds containing carboxyl groups, the doubly-bound oxygen atom of a carboxyl group being replaced by a doubly-bound nitrogen atom, this nitrogen atom not being further bound to an oxygen atom, e.g. imino-ethers, amidines
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D235/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings
- C07D235/02—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings condensed with carbocyclic rings or ring systems
- C07D235/04—Benzimidazoles; Hydrogenated benzimidazoles
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Engineering & Computer Science (AREA)
- Diabetes (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Hematology (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Preventing Corrosion Or Incrustation Of Metals (AREA)
- Separation Of Suspended Particles By Flocculating Agents (AREA)
Abstract
A találmány tárgyát az (I) általánős képletű, naftilcsőpőrttalszűbsztitűált benzimidazől-származékők - a képletben A jelentésealkilén-, karbőnil- vagy szűlfőnilcsőpőrt, R1 jelentése hidrőgénatőm,-.OR5 vagy -N(R5) R6 általánős képletű csőpőrt, R2 jelentése nitrő-,adőtt esetben szűbsztitűált alkil- vagy heterőciklűsős csőpőrt, R3jelentése hidrőgénatőm, adőtt esetben szűbsztitűált alkil-, aril-őxi-,aralkil-őxi-, alkenil-, ciklőalkil-, imidazőlil-, indőlil- vagyadamantilcsőpőrt, -C(O)OR8, -N(R8)R9, -C(O)N(R8)R)9, -R9, -N(R8)C(O)N(R8)R9, -N(R8)C(NH)N(R8)R9, -OPO3H2 vagy -SR8 általánősképletű csőpőrt, R4 jelentése -C(NH)N(-R8)R9, -C(NH)N(H)OR8, -C(NH)N(H)C(O)R8 vagy -C(NH)N(H)C(O)OR8 általánős képletű csőpőrt, nértéke 0, 1, 2 vagy 3- és gyógyszerészetileg elfőgadható sóik képezik.A vegyületek véralvadás-kaszkádban a Xa és a Ila (trőmbin) faktőrőkatgátőlják, és ezáltal véralvadás-gátlóként használhatók. ŕ
Applications Claiming Priority (2)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US08/570,057 US5849759A (en) | 1995-12-08 | 1995-12-08 | Naphthyl-substituted benzimidazole derivatives as anti-coagulants |
PCT/IB1996/001496 WO1997021437A1 (en) | 1995-12-08 | 1996-12-05 | Naphthyl-substituted benzimidazole derivatives as anticoagulants |
Publications (2)
Publication Number | Publication Date |
---|---|
HUP9904066A2 true HUP9904066A2 (hu) | 2000-03-28 |
HUP9904066A3 HUP9904066A3 (en) | 2001-11-28 |
Family
ID=24278023
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
HU9904066A HUP9904066A3 (en) | 1995-12-08 | 1996-12-05 | Naphthyl-substituted benzimidazole derivatives as anticoagulants and use thereof |
Country Status (23)
Country | Link |
---|---|
US (1) | US5849759A (hu) |
EP (1) | EP0865281B1 (hu) |
JP (1) | JP2000502082A (hu) |
KR (1) | KR19990071974A (hu) |
CN (1) | CN1110305C (hu) |
AT (1) | ATE215371T1 (hu) |
CZ (1) | CZ177698A3 (hu) |
DE (1) | DE69620443T2 (hu) |
DK (1) | DK0865281T3 (hu) |
ES (1) | ES2175179T3 (hu) |
HK (1) | HK1018208A1 (hu) |
HU (1) | HUP9904066A3 (hu) |
IL (1) | IL124537A (hu) |
MX (1) | MX9804597A (hu) |
NO (1) | NO312673B1 (hu) |
NZ (1) | NZ325449A (hu) |
PL (1) | PL327169A1 (hu) |
PT (1) | PT865281E (hu) |
RU (1) | RU98112597A (hu) |
SK (1) | SK282767B6 (hu) |
UA (1) | UA49869C2 (hu) |
WO (1) | WO1997021437A1 (hu) |
ZA (1) | ZA9610315B (hu) |
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TW201813963A (zh) | 2016-09-23 | 2018-04-16 | 美商基利科學股份有限公司 | 磷脂醯肌醇3-激酶抑制劑 |
WO2018151873A1 (en) | 2017-02-16 | 2018-08-23 | Arena Pharmaceuticals, Inc. | Compounds and methods for treatment of primary biliary cholangitis |
MX2022000133A (es) | 2019-07-01 | 2022-04-27 | Tonix Pharma Ltd | Anticuerpos anti-cd154 y usos de los mismos. |
US20240059781A1 (en) | 2021-01-06 | 2024-02-22 | Tonix Pharma Limited | Methods of inducing immune tolerance with modified anti-cd154 antibodies |
Family Cites Families (9)
Publication number | Priority date | Publication date | Assignee | Title |
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JPS59139357A (ja) * | 1983-01-28 | 1984-08-10 | Torii Yakuhin Kk | アミジン誘導体 |
ZA928276B (en) * | 1991-10-31 | 1993-05-06 | Daiichi Seiyaku Co | Aromatic amidine derivates and salts thereof. |
WO1993015756A1 (en) * | 1992-02-14 | 1993-08-19 | Corvas International, Inc. | Inhibitors of thrombosis |
US5492895A (en) * | 1992-02-14 | 1996-02-20 | Corvas International, Inc. | Inhibitors of thrombosis |
DE4213919A1 (de) * | 1992-04-28 | 1993-11-04 | Thomae Gmbh Dr K | Cyclische iminoderivate, verfahren zu ihrer herstellung und diese verbindungen enthaltende arzneimittel |
AU675981B2 (en) * | 1992-12-02 | 1997-02-27 | Bristol-Myers Squibb Company | Guanidinyl-substituted heterocyclic thrombin inhibitors |
JPH08504769A (ja) * | 1992-12-15 | 1996-05-21 | コルバス・インターナショナル、インコーポレイテッド | 因子Xaの新規インヒビター |
US5332822A (en) * | 1992-12-24 | 1994-07-26 | Bristol-Myers Squibb Company | Heteroaromatic and thioheteroaromatic substituted sulfonamide thrombin inhibitors |
IL113472A0 (en) * | 1994-04-29 | 1995-07-31 | Lilly Co Eli | Non-peptidyl tachykinin receptor antogonists |
-
1995
- 1995-12-08 US US08/570,057 patent/US5849759A/en not_active Expired - Fee Related
-
1996
- 1996-12-05 ES ES96944123T patent/ES2175179T3/es not_active Expired - Lifetime
- 1996-12-05 NZ NZ325449A patent/NZ325449A/xx unknown
- 1996-12-05 DK DK96944123T patent/DK0865281T3/da active
- 1996-12-05 SK SK746-98A patent/SK282767B6/sk unknown
- 1996-12-05 PT PT96944123T patent/PT865281E/pt unknown
- 1996-12-05 WO PCT/IB1996/001496 patent/WO1997021437A1/en not_active Application Discontinuation
- 1996-12-05 IL IL12453796A patent/IL124537A/en not_active IP Right Cessation
- 1996-12-05 AT AT96944123T patent/ATE215371T1/de not_active IP Right Cessation
- 1996-12-05 MX MX9804597A patent/MX9804597A/es not_active IP Right Cessation
- 1996-12-05 CZ CZ981776A patent/CZ177698A3/cs unknown
- 1996-12-05 PL PL96327169A patent/PL327169A1/xx unknown
- 1996-12-05 CN CN96199921A patent/CN1110305C/zh not_active Expired - Fee Related
- 1996-12-05 DE DE69620443T patent/DE69620443T2/de not_active Expired - Fee Related
- 1996-12-05 UA UA98073607A patent/UA49869C2/uk unknown
- 1996-12-05 KR KR1019980704265A patent/KR19990071974A/ko not_active Application Discontinuation
- 1996-12-05 HU HU9904066A patent/HUP9904066A3/hu unknown
- 1996-12-05 EP EP96944123A patent/EP0865281B1/en not_active Expired - Lifetime
- 1996-12-05 JP JP9521899A patent/JP2000502082A/ja not_active Ceased
- 1996-12-05 RU RU98112597/04A patent/RU98112597A/ru not_active Application Discontinuation
- 1996-12-06 ZA ZA9610315A patent/ZA9610315B/xx unknown
-
1998
- 1998-06-05 NO NO19982606A patent/NO312673B1/no unknown
-
1999
- 1999-07-27 HK HK99103225A patent/HK1018208A1/xx not_active IP Right Cessation
Also Published As
Publication number | Publication date |
---|---|
NO982606L (no) | 1998-08-10 |
IL124537A0 (en) | 1998-12-06 |
EP0865281A1 (en) | 1998-09-23 |
UA49869C2 (uk) | 2002-10-15 |
MX9804597A (es) | 1998-10-31 |
KR19990071974A (ko) | 1999-09-27 |
ATE215371T1 (de) | 2002-04-15 |
AU1395697A (en) | 1997-07-03 |
DE69620443T2 (de) | 2002-11-28 |
RU98112597A (ru) | 2000-10-20 |
EP0865281A4 (en) | 1999-07-28 |
ZA9610315B (en) | 1997-06-17 |
EP0865281B1 (en) | 2002-04-03 |
SK282767B6 (sk) | 2002-12-03 |
JP2000502082A (ja) | 2000-02-22 |
NZ325449A (en) | 2000-01-28 |
CZ177698A3 (cs) | 1998-09-16 |
ES2175179T3 (es) | 2002-11-16 |
DE69620443D1 (de) | 2002-05-08 |
PL327169A1 (en) | 1998-11-23 |
IL124537A (en) | 2002-04-21 |
PT865281E (pt) | 2002-09-30 |
DK0865281T3 (da) | 2002-07-29 |
HUP9904066A3 (en) | 2001-11-28 |
US5849759A (en) | 1998-12-15 |
CN1110305C (zh) | 2003-06-04 |
NO982606D0 (no) | 1998-06-05 |
SK74698A3 (en) | 1998-12-02 |
CN1209062A (zh) | 1999-02-24 |
WO1997021437A1 (en) | 1997-06-19 |
HK1018208A1 (en) | 1999-12-17 |
AU700894B2 (en) | 1999-01-14 |
NO312673B1 (no) | 2002-06-17 |
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