BRPI0512084A - heterociclos de cinco membros úteis como inibidores de serina protease, composição farmacêutica contendo os mesmos, bem como seu uso - Google Patents
heterociclos de cinco membros úteis como inibidores de serina protease, composição farmacêutica contendo os mesmos, bem como seu usoInfo
- Publication number
- BRPI0512084A BRPI0512084A BRPI0512084-5A BRPI0512084A BRPI0512084A BR PI0512084 A BRPI0512084 A BR PI0512084A BR PI0512084 A BRPI0512084 A BR PI0512084A BR PI0512084 A BRPI0512084 A BR PI0512084A
- Authority
- BR
- Brazil
- Prior art keywords
- factor
- formula
- serine protease
- compounds
- pharmaceutical compositions
- Prior art date
Links
- 239000008194 pharmaceutical composition Substances 0.000 title abstract 3
- 239000003001 serine protease inhibitor Substances 0.000 title abstract 2
- 125000000623 heterocyclic group Chemical group 0.000 title 1
- 150000001875 compounds Chemical class 0.000 abstract 5
- 108010048049 Factor IXa Proteins 0.000 abstract 1
- 108010080805 Factor XIa Proteins 0.000 abstract 1
- 108010074860 Factor Xa Proteins 0.000 abstract 1
- 102000003827 Plasma Kallikrein Human genes 0.000 abstract 1
- 108090000113 Plasma Kallikrein Proteins 0.000 abstract 1
- 229940124639 Selective inhibitor Drugs 0.000 abstract 1
- 108010022999 Serine Proteases Proteins 0.000 abstract 1
- 102000012479 Serine Proteases Human genes 0.000 abstract 1
- 108090000190 Thrombin Proteins 0.000 abstract 1
- 208000007536 Thrombosis Diseases 0.000 abstract 1
- 230000004913 activation Effects 0.000 abstract 1
- 230000015271 coagulation Effects 0.000 abstract 1
- 238000005345 coagulation Methods 0.000 abstract 1
- 208000027866 inflammatory disease Diseases 0.000 abstract 1
- 239000003112 inhibitor Substances 0.000 abstract 1
- 238000000034 method Methods 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 239000012453 solvate Substances 0.000 abstract 1
- 229960004072 thrombin Drugs 0.000 abstract 1
- 230000001732 thrombotic effect Effects 0.000 abstract 1
Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
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- C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
- C07D417/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings
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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
- A61K31/41—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
- A61K31/4164—1,3-Diazoles
- A61K31/4178—1,3-Diazoles not condensed 1,3-diazoles and containing further heterocyclic rings, e.g. pilocarpine, nitrofurantoin
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
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- 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
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- A—HUMAN NECESSITIES
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- 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
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- 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
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- A—HUMAN NECESSITIES
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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- A61P9/06—Antiarrhythmics
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- 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
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- C07D231/00—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
- C07D231/02—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings
- C07D231/10—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
- C07D231/12—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
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- 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
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- C07D235/06—Benzimidazoles; Hydrogenated benzimidazoles with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached in position 2
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- C07D249/00—Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms
- C07D249/02—Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms not condensed with other rings
- C07D249/08—1,2,4-Triazoles; Hydrogenated 1,2,4-triazoles
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- C07D249/08—1,2,4-Triazoles; Hydrogenated 1,2,4-triazoles
- C07D249/10—1,2,4-Triazoles; Hydrogenated 1,2,4-triazoles 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
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- C07D263/12—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms with radicals containing only hydrogen and carbon atoms
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- C07D263/10—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
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- C07D263/30—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
- C07D263/32—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
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- C07D401/04—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 directly linked by a ring-member-to-ring-member bond
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- C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
- C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
- C07D417/06—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
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Applications Claiming Priority (4)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US57963804P | 2004-06-15 | 2004-06-15 | |
| US68412705P | 2005-05-24 | 2005-05-24 | |
| US11/151,667 US7453002B2 (en) | 2004-06-15 | 2005-06-13 | Five-membered heterocycles useful as serine protease inhibitors |
| PCT/US2005/021212 WO2005123050A2 (en) | 2004-06-15 | 2005-06-14 | Five-membered heterocycles useful as serine protease inhibitors |
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| Publication Number | Publication Date |
|---|---|
| BRPI0512084A true BRPI0512084A (pt) | 2008-02-06 |
Family
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Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| BRPI0512084-5A BRPI0512084A (pt) | 2004-06-15 | 2005-06-14 | heterociclos de cinco membros úteis como inibidores de serina protease, composição farmacêutica contendo os mesmos, bem como seu uso |
Country Status (13)
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| US (6) | US7453002B2 (https=) |
| EP (1) | EP1773786B1 (https=) |
| JP (1) | JP4791460B2 (https=) |
| KR (1) | KR20070024601A (https=) |
| AU (1) | AU2005254102A1 (https=) |
| BR (1) | BRPI0512084A (https=) |
| CA (1) | CA2570472A1 (https=) |
| ES (1) | ES2628279T3 (https=) |
| IL (1) | IL179844A0 (https=) |
| MX (1) | MXPA06014642A (https=) |
| NO (1) | NO20065864L (https=) |
| RU (1) | RU2007101073A (https=) |
| WO (1) | WO2005123050A2 (https=) |
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-
2005
- 2005-06-13 US US11/151,667 patent/US7453002B2/en active Active
- 2005-06-14 BR BRPI0512084-5A patent/BRPI0512084A/pt not_active IP Right Cessation
- 2005-06-14 CA CA002570472A patent/CA2570472A1/en not_active Abandoned
- 2005-06-14 JP JP2007516703A patent/JP4791460B2/ja not_active Expired - Fee Related
- 2005-06-14 WO PCT/US2005/021212 patent/WO2005123050A2/en not_active Ceased
- 2005-06-14 MX MXPA06014642A patent/MXPA06014642A/es active IP Right Grant
- 2005-06-14 KR KR1020067026365A patent/KR20070024601A/ko not_active Ceased
- 2005-06-14 RU RU2007101073/04A patent/RU2007101073A/ru not_active Application Discontinuation
- 2005-06-14 ES ES05773261.2T patent/ES2628279T3/es not_active Expired - Lifetime
- 2005-06-14 EP EP05773261.2A patent/EP1773786B1/en not_active Expired - Lifetime
- 2005-06-14 AU AU2005254102A patent/AU2005254102A1/en not_active Abandoned
-
2006
- 2006-12-05 IL IL179844A patent/IL179844A0/en unknown
- 2006-12-15 NO NO20065864A patent/NO20065864L/no not_active Application Discontinuation
-
2008
- 2008-09-12 US US12/209,235 patent/US8101778B2/en active Active
-
2011
- 2011-12-15 US US13/326,809 patent/US8716492B2/en not_active Expired - Lifetime
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2014
- 2014-03-19 US US14/219,311 patent/US9079860B2/en not_active Expired - Lifetime
-
2015
- 2015-05-27 US US14/722,434 patent/US9617224B2/en not_active Expired - Lifetime
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2017
- 2017-02-23 US US15/440,346 patent/US10112936B2/en not_active Expired - Lifetime
Also Published As
| Publication number | Publication date |
|---|---|
| JP2008502700A (ja) | 2008-01-31 |
| WO2005123050A2 (en) | 2005-12-29 |
| NO20065864L (no) | 2007-03-02 |
| ES2628279T3 (es) | 2017-08-02 |
| IL179844A0 (en) | 2007-07-04 |
| AU2005254102A1 (en) | 2005-12-29 |
| JP4791460B2 (ja) | 2011-10-12 |
| CA2570472A1 (en) | 2005-12-29 |
| KR20070024601A (ko) | 2007-03-02 |
| WO2005123050A3 (en) | 2007-01-04 |
| US7453002B2 (en) | 2008-11-18 |
| US9079860B2 (en) | 2015-07-14 |
| US8716492B2 (en) | 2014-05-06 |
| MXPA06014642A (es) | 2007-02-12 |
| US8101778B2 (en) | 2012-01-24 |
| US20120088758A1 (en) | 2012-04-12 |
| US20150259297A1 (en) | 2015-09-17 |
| US20140206706A1 (en) | 2014-07-24 |
| US10112936B2 (en) | 2018-10-30 |
| EP1773786A2 (en) | 2007-04-18 |
| US20050282805A1 (en) | 2005-12-22 |
| US20090036438A1 (en) | 2009-02-05 |
| US20170166560A1 (en) | 2017-06-15 |
| US9617224B2 (en) | 2017-04-11 |
| EP1773786B1 (en) | 2017-04-26 |
| RU2007101073A (ru) | 2008-07-20 |
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