JP2010531353A5 - - Google Patents
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- JP2010531353A5 JP2010531353A5 JP2010514672A JP2010514672A JP2010531353A5 JP 2010531353 A5 JP2010531353 A5 JP 2010531353A5 JP 2010514672 A JP2010514672 A JP 2010514672A JP 2010514672 A JP2010514672 A JP 2010514672A JP 2010531353 A5 JP2010531353 A5 JP 2010531353A5
- Authority
- JP
- Japan
- Prior art keywords
- thrombin
- group
- plasma
- hydrogen
- pharmaceutically acceptable
- 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.)
- Pending
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- 108090000190 Thrombin Proteins 0.000 claims description 78
- 229960004072 thrombin Drugs 0.000 claims description 77
- 150000001875 compounds Chemical class 0.000 claims description 66
- 230000015271 coagulation Effects 0.000 claims description 28
- 238000005345 coagulation Methods 0.000 claims description 28
- 239000003146 anticoagulant agent Substances 0.000 claims description 26
- 150000003839 salts Chemical class 0.000 claims description 21
- 229940127219 anticoagulant drug Drugs 0.000 claims description 19
- 229910052739 hydrogen Inorganic materials 0.000 claims description 18
- 239000001257 hydrogen Substances 0.000 claims description 18
- 239000003058 plasma substitute Substances 0.000 claims description 14
- 239000012453 solvate Substances 0.000 claims description 13
- 150000002431 hydrogen Chemical class 0.000 claims description 11
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 claims description 9
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims description 7
- 208000007536 Thrombosis Diseases 0.000 claims description 7
- 229910052736 halogen Inorganic materials 0.000 claims description 7
- 150000002367 halogens Chemical class 0.000 claims description 7
- 230000002401 inhibitory effect Effects 0.000 claims description 7
- 125000004191 (C1-C6) alkoxy group Chemical group 0.000 claims description 6
- 125000000217 alkyl group Chemical group 0.000 claims description 6
- 239000003937 drug carrier Substances 0.000 claims description 4
- 239000008194 pharmaceutical composition Substances 0.000 claims description 4
- 206010059484 Haemodilution Diseases 0.000 claims description 3
- 241000124008 Mammalia Species 0.000 claims description 3
- 230000002265 prevention Effects 0.000 claims description 3
- 206010020850 Hyperthyroidism Diseases 0.000 claims description 2
- 125000000499 benzofuranyl group Chemical group O1C(=CC2=C1C=CC=C2)* 0.000 claims description 2
- 125000004196 benzothienyl group Chemical group S1C(=CC2=C1C=CC=C2)* 0.000 claims description 2
- 230000001419 dependent effect Effects 0.000 claims description 2
- 125000002541 furyl group Chemical group 0.000 claims description 2
- 125000001041 indolyl group Chemical group 0.000 claims description 2
- 125000002971 oxazolyl group Chemical group 0.000 claims description 2
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims description 2
- 125000003373 pyrazinyl group Chemical group 0.000 claims description 2
- 125000002098 pyridazinyl group Chemical group 0.000 claims description 2
- 125000004076 pyridyl group Chemical group 0.000 claims description 2
- 125000000714 pyrimidinyl group Chemical group 0.000 claims description 2
- 125000001424 substituent group Chemical group 0.000 claims description 2
- 125000000335 thiazolyl group Chemical group 0.000 claims description 2
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- RTZKZFJDLAIYFH-UHFFFAOYSA-N Diethyl ether Chemical compound CCOCC RTZKZFJDLAIYFH-UHFFFAOYSA-N 0.000 description 17
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- MNURPFVONZPVLA-UHFFFAOYSA-N 2-chlorobenzenesulfonic acid Chemical compound OS(=O)(=O)C1=CC=CC=C1Cl MNURPFVONZPVLA-UHFFFAOYSA-N 0.000 description 5
- XGWZKPKLPOKIRV-UHFFFAOYSA-N 3-amino-n-methyl-4-(methylamino)-n-phenylbenzenesulfonamide Chemical compound C1=C(N)C(NC)=CC=C1S(=O)(=O)N(C)C1=CC=CC=C1 XGWZKPKLPOKIRV-UHFFFAOYSA-N 0.000 description 5
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- 102000004506 Blood Proteins Human genes 0.000 description 5
- 108010017384 Blood Proteins Proteins 0.000 description 5
- 108010000499 Thromboplastin Proteins 0.000 description 5
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- 238000009825 accumulation Methods 0.000 description 5
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- SRSXLGNVWSONIS-UHFFFAOYSA-N benzenesulfonic acid Chemical compound OS(=O)(=O)C1=CC=CC=C1 SRSXLGNVWSONIS-UHFFFAOYSA-N 0.000 description 5
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- PGOHTUIFYSHAQG-LJSDBVFPSA-N (2S)-6-amino-2-[[(2S)-5-amino-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-4-amino-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-5-amino-2-[[(2S)-5-amino-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S,3R)-2-[[(2S)-5-amino-2-[[(2S)-2-[[(2S)-2-[[(2S,3R)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-5-amino-2-[[(2S)-1-[(2S,3R)-2-[[(2S)-2-[[(2S)-2-[[(2R)-2-[[(2S)-2-[[(2S)-2-[[2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-1-[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-amino-4-methylsulfanylbutanoyl]amino]-3-(1H-indol-3-yl)propanoyl]amino]-5-carbamimidamidopentanoyl]amino]propanoyl]pyrrolidine-2-carbonyl]amino]-3-methylbutanoyl]amino]-4-methylpentanoyl]amino]-4-methylpentanoyl]amino]acetyl]amino]-3-hydroxypropanoyl]amino]-4-methylpentanoyl]amino]-3-sulfanylpropanoyl]amino]-4-methylsulfanylbutanoyl]amino]-5-carbamimidamidopentanoyl]amino]-3-hydroxybutanoyl]pyrrolidine-2-carbonyl]amino]-5-oxopentanoyl]amino]-3-hydroxypropanoyl]amino]-3-hydroxypropanoyl]amino]-3-(1H-imidazol-5-yl)propanoyl]amino]-4-methylpentanoyl]amino]-3-hydroxybutanoyl]amino]-3-(1H-indol-3-yl)propanoyl]amino]-5-carbamimidamidopentanoyl]amino]-5-oxopentanoyl]amino]-3-hydroxybutanoyl]amino]-3-hydroxypropanoyl]amino]-3-carboxypropanoyl]amino]-3-hydroxypropanoyl]amino]-5-oxopentanoyl]amino]-5-oxopentanoyl]amino]-3-phenylpropanoyl]amino]-5-carbamimidamidopentanoyl]amino]-3-methylbutanoyl]amino]-4-methylpentanoyl]amino]-4-oxobutanoyl]amino]-5-carbamimidamidopentanoyl]amino]-3-(1H-indol-3-yl)propanoyl]amino]-4-carboxybutanoyl]amino]-5-oxopentanoyl]amino]hexanoic acid Chemical compound CSCC[C@H](N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCNC(N)=N)C(=O)N[C@@H](C)C(=O)N1CCC[C@H]1C(=O)N[C@@H](C(C)C)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(C)C)C(=O)NCC(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CS)C(=O)N[C@@H](CCSC)C(=O)N[C@@H](CCCNC(N)=N)C(=O)N[C@@H]([C@@H](C)O)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CO)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H]([C@@H](C)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCNC(N)=N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H]([C@@H](C)O)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(O)=O)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(N)=N)C(=O)N[C@@H](C(C)C)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCCNC(N)=N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCC(O)=O)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCCN)C(O)=O PGOHTUIFYSHAQG-LJSDBVFPSA-N 0.000 description 4
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| UA75093C2 (en) * | 2000-10-06 | 2006-03-15 | Dimensional Pharm Inc | Aminopyridinyl-,aminoguanidinyl-, and alkoxyguanidinesubstituted phenylsubstituted phenylacetamides as protease inhibitors |
| JP4896387B2 (ja) * | 2003-09-30 | 2012-03-14 | 武田薬品工業株式会社 | チアゾリン誘導体およびその用途 |
| AU2005229505B2 (en) * | 2004-03-02 | 2010-07-15 | F. Hoffmann-La Roche Ag | 4- (sulfanyl-pyrimidin-4-ylmethyl) -morpholine derivatives and related compounds as GABA receptor ligands for the treatment of anxiety, depression and epilepsy |
| RU2300385C1 (ru) * | 2005-12-27 | 2007-06-10 | Елена Ивановна Синауридзе | Раствор для коррекции первичных нарушений гемостаза плазмозамещающими растворами нового состава |
| CA2647597A1 (en) * | 2006-05-31 | 2007-12-06 | Abbott Laboratories | Thiazole compounds as cannabinoid receptor ligands and uses thereof |
| RU2353619C2 (ru) * | 2007-06-28 | 2009-04-27 | Общество С Ограниченной Ответственностью "Бионика" | Новые соединения, обладающие функцией антикоагулянтов, фармацевтические композиции на их основе для лечения тромботических состояний и плазмозамещающий раствор для коррекции гиперкоагуляционных нарушений при гемодилюции |
| RU2354647C2 (ru) * | 2007-06-28 | 2009-05-10 | Общество С Ограниченной Ответственностью "Бионика" | Новые соединения, обладающие функцией ингибиторов тромбина, и фармацевтические композиции на их основе |
-
2007
- 2007-06-28 RU RU2007124202/04A patent/RU2353619C2/ru not_active IP Right Cessation
-
2008
- 2008-06-27 AU AU2008269258A patent/AU2008269258B2/en not_active Ceased
- 2008-06-27 EP EP08794029A patent/EP2178839A2/en not_active Withdrawn
- 2008-06-27 KR KR1020107002061A patent/KR20100028122A/ko not_active Abandoned
- 2008-06-27 US US12/666,250 patent/US8426433B2/en not_active Expired - Fee Related
- 2008-06-27 CA CA002692363A patent/CA2692363A1/en not_active Abandoned
- 2008-06-27 UA UAA201000790A patent/UA98969C2/ru unknown
- 2008-06-27 EA EA201000064A patent/EA020915B1/ru not_active IP Right Cessation
- 2008-06-27 JP JP2010514672A patent/JP2010531353A/ja active Pending
- 2008-06-27 WO PCT/RU2008/000401 patent/WO2009002229A2/en not_active Ceased
- 2008-06-27 CN CN200880104823.1A patent/CN101848894B/zh not_active Expired - Fee Related
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