SI9620136B - Substituted n-/(aminoiminomethyl or aminomethyl)phenyl/-propyl amides - Google Patents
Substituted n-/(aminoiminomethyl or aminomethyl)phenyl/-propyl amides Download PDFInfo
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- SI9620136B SI9620136B SI9620136A SI9620136A SI9620136B SI 9620136 B SI9620136 B SI 9620136B SI 9620136 A SI9620136 A SI 9620136A SI 9620136 A SI9620136 A SI 9620136A SI 9620136 B SI9620136 B SI 9620136B
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- pharmaceutically acceptable
- acceptable salt
- optionally substituted
- alkyl
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- 0 CC(C(Cc1cccc([N+]([N-])N)c1)C(OC)=O)N*(c1ccc2[n]ccc2c1)=O Chemical compound CC(C(Cc1cccc([N+]([N-])N)c1)C(OC)=O)N*(c1ccc2[n]ccc2c1)=O 0.000 description 8
- AXCHQMQEQBQLSQ-UHFFFAOYSA-N CC(NCc(cc1)ccc1-c(cc1)ccc1C(NC(Cc1ccccc1)C(Cc1cccc(C(N)=N)c1)CO)=O)=O Chemical compound CC(NCc(cc1)ccc1-c(cc1)ccc1C(NC(Cc1ccccc1)C(Cc1cccc(C(N)=N)c1)CO)=O)=O AXCHQMQEQBQLSQ-UHFFFAOYSA-N 0.000 description 1
- IHZLJQJUXBWDQX-UHFFFAOYSA-N CC(OCC(Cc1cccc(C(N)=N)c1)C(CCc1ccccc1)NC(c(cc1)ccc1-c(cc1)ccc1F)=O)=O Chemical compound CC(OCC(Cc1cccc(C(N)=N)c1)C(CCc1ccccc1)NC(c(cc1)ccc1-c(cc1)ccc1F)=O)=O IHZLJQJUXBWDQX-UHFFFAOYSA-N 0.000 description 1
- NDHZTNQUDAISTQ-UHFFFAOYSA-N CC(OCC(Cc1cccc(C(N)=N)c1)C(CCc1ccccc1)NC(c(cc1)ccc1-c1ccc2OCOc2c1)=O)=O Chemical compound CC(OCC(Cc1cccc(C(N)=N)c1)C(CCc1ccccc1)NC(c(cc1)ccc1-c1ccc2OCOc2c1)=O)=O NDHZTNQUDAISTQ-UHFFFAOYSA-N 0.000 description 1
- OFIYMQGJSZIJHB-UHFFFAOYSA-N CC(OCC(Cc1cccc(C(N)=N)c1)C(CCc1ccccc1)NC(c(cc1)ccc1-c1cccc(F)c1)=O)=O Chemical compound CC(OCC(Cc1cccc(C(N)=N)c1)C(CCc1ccccc1)NC(c(cc1)ccc1-c1cccc(F)c1)=O)=O OFIYMQGJSZIJHB-UHFFFAOYSA-N 0.000 description 1
- GIPDSDBNHZKLJJ-UHFFFAOYSA-N CCC(C)C(C(Cc1cccc(C(N)=N)c1)CO)NC(c(cc1)ccc1-c1cccc(CN)c1)=O Chemical compound CCC(C)C(C(Cc1cccc(C(N)=N)c1)CO)NC(c(cc1)ccc1-c1cccc(CN)c1)=O GIPDSDBNHZKLJJ-UHFFFAOYSA-N 0.000 description 1
- RZCGFKOLPIVLDE-UHFFFAOYSA-N COC(C(Cc1cccc(C(N)=N)c1)C(Cc1ccccc1)NC(c(cc1)ccc1-c1ccccc1)=O)=O Chemical compound COC(C(Cc1cccc(C(N)=N)c1)C(Cc1ccccc1)NC(c(cc1)ccc1-c1ccccc1)=O)=O RZCGFKOLPIVLDE-UHFFFAOYSA-N 0.000 description 1
- WZWIBZRDPCGVOJ-UHFFFAOYSA-N NC(c1cc(CC(CO)C(CCc2ccccc2)NC(c(cc2)ccc2-c(cc2)ccc2F)=O)ccc1)=N Chemical compound NC(c1cc(CC(CO)C(CCc2ccccc2)NC(c(cc2)ccc2-c(cc2)ccc2F)=O)ccc1)=N WZWIBZRDPCGVOJ-UHFFFAOYSA-N 0.000 description 1
- OXNJTTYOCUHODK-UHFFFAOYSA-N NC(c1cc(CC(CO)C(Cc2ccccc2)NC(c(cc2)ccc2-c2cccc(O)c2)=O)ccc1)=N Chemical compound NC(c1cc(CC(CO)C(Cc2ccccc2)NC(c(cc2)ccc2-c2cccc(O)c2)=O)ccc1)=N OXNJTTYOCUHODK-UHFFFAOYSA-N 0.000 description 1
- QRJFGWOXDCNDBD-UHFFFAOYSA-N NCc1cc(-c(cc2)ccc2C(NC(C(Cc2cc(C(N)=N)ccc2)CO)c2cnccc2)=O)ccc1 Chemical compound NCc1cc(-c(cc2)ccc2C(NC(C(Cc2cc(C(N)=N)ccc2)CO)c2cnccc2)=O)ccc1 QRJFGWOXDCNDBD-UHFFFAOYSA-N 0.000 description 1
- RWNGKDOQYSYPDY-UHFFFAOYSA-N NCc1cc(-c(cc2)ccc2C(NC(Cc2ccccc2)C(Cc2cccc(C(N)=N)c2)CO)=O)ccc1 Chemical compound NCc1cc(-c(cc2)ccc2C(NC(Cc2ccccc2)C(Cc2cccc(C(N)=N)c2)CO)=O)ccc1 RWNGKDOQYSYPDY-UHFFFAOYSA-N 0.000 description 1
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- C07D207/30—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having two double bonds between ring members or between ring members and non-ring members
- C07D207/32—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having two 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
- C07D207/325—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having two 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 with substituted hydrocarbon radicals directly attached to the ring nitrogen atom
- C07D207/327—Radicals substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
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- C07C255/60—Carboxylic acid nitriles having cyano groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton containing cyano groups and singly-bound nitrogen atoms, not being further bound to other hetero atoms, bound to the carbon skeleton at least one of the singly-bound nitrogen atoms being acylated
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- 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
- C07C257/10—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 with replacement of the other oxygen atom of the carboxyl group by nitrogen atoms, e.g. amidines
- C07C257/18—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 with replacement of the other oxygen atom of the carboxyl group by nitrogen atoms, e.g. amidines having carbon atoms of amidino groups bound to carbon atoms of six-membered aromatic rings
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- C07C259/12—Compounds containing carboxyl groups, an oxygen atom of a carboxyl group being replaced by a nitrogen atom, this nitrogen atom being further bound to an oxygen atom and not being part of nitro or nitroso groups with replacement of the other oxygen atom of the carboxyl group by nitrogen atoms, e.g. N-hydroxyamidines
- C07C259/18—Compounds containing carboxyl groups, an oxygen atom of a carboxyl group being replaced by a nitrogen atom, this nitrogen atom being further bound to an oxygen atom and not being part of nitro or nitroso groups with replacement of the other oxygen atom of the carboxyl group by nitrogen atoms, e.g. N-hydroxyamidines having carbon atoms of hydroxamidine groups bound to carbon atoms of six-membered aromatic rings
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- C07D249/04—1,2,3-Triazoles; Hydrogenated 1,2,3-triazoles
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- C07D277/32—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members 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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Claims (24)
- Λ Patentni zahtevki 1. Spojina s formuloRi in R2 sta vodik ali skupaj =NRg; R3 je -C02R6, -C(0)R6, -CONR^R*, -CH2OR7 ali -CH2SR7; R4 je skupina s formulo:ali je R4 vodik, alkil, cikloalkil ali cikloalkilalkil; R5 je alkil, alkenil, po izbiri substituiran aril ali po izbiri substituiran heteroaril; R<5 je vodik ali C^alkil; R7 je vodik, C^alkil, Ci.7acil, aroil ali heteroaril; R8 je vodik ali Ci_6alkil; Roje Ri0O2C-, R10O-, HO-, ciano, Ri0CO-, HCO-, Ci^alkil, nitro ali Υ^Ν-, kjer je Rio po izbiri substituiran alkil, po izbiri substituiran aralkil ali po izbiri substituiran heteroaralkil in kjer sta Υ1 in Y2 neodvisno vodik ali alkil; A in B sta vodik ali skupaj vez; Ar je po izbiri substituiran aril ali po izbiri substituiran heteroaril in n je 0, 1 ali 2, ali njena farmacevtsko sprejemljiva sol, njen N-oksid, njen hidrat ali njen solvat. 2-
- 2. Spojina po zahtevku 1, označena s tem, da sta Rj in R2 skupaj =NH.
- 3. Spojina po zahtevku 2, označena s tem, da sta Ri in R2 skupaj =NH in tvorita aminoiminometil na fenilnem delu, ki je v meta položaju glede na položaj vezave fenilnega dela na propilnem delu.
- 4. Spojina po zahtevku 1, označena s tem, daje R3 -C02R$, -CH2OR7 ali -CH2SR7.
- 5. Spojina po zahtevku 4, označena s tem, daje R3 -C02R$ in je R$ Ci^alkil.
- 6. Spojina po zahtevku 4, označena s tem, da je R3 -CH2OR7 ali -CH2SR7 in je R7 vodik ali Ci.6alkil.
- 7. Spojina po zahtevku 1, označena s tem, daje n 1.
- 8. Spojina po zahtevku 1, označena s tem, daje Ar po izbiri substituiran aril.
- 9. Spojina po zahtevku 1, označena s tem, daje Ar fenil.
- 10. Spojina po zahtevku 1, označena s tem, da je R5 po izbiri substituiran fenil, po izbiri substituiran bifenil, po izbiri substituiran naftil ali po izbiri substituiran heterobifenil.
- 11. Spojina po zahtevku 1, označena s tem, daje: 3η2ν^ COOMe Η2Ν P*» ΝΗ ΗΝ /=\ >ocη2νγ^νη. F8ο2ν η2ν5NHAcΗ2ΝΓ ^NH. H2N^NH. 40ΓΛιΓΛο ΝΗ ΟΑΑ OMe ΝΗ ΝΗ243 0-0^° '—' ΝΗ Ο \* Ν-λ * οPh' °Μβ ΝΗ ΝΗ, ΝΗ Ο Ph-~^-^v*A V' £ °Me ΝΗ "Ό^ b-Oi ali ΝΗ Ο Ph '0H ΝΗ ali njena farmacevtsko sprejemljiva sol.
- 12. Farmacevtski sestavek, označen s tem, da obsega farmacevtsko sprejemljivo količino spojine po zahtevku 1 in farmacevtsko sprejemljiv nosilec.
- 13. Uporaba farmacevtsko učinkovite količine spojine po zahtevku 1 ali njene farmacevtsko sprejemljive soli za izdelavo zdravila za zdravljenje patološkega učinka trombina.
- 14. Uporaba farmacevtsko učinkovite količine spojine po zahtevku 1 ali njene farmacevtsko sprejemljive soli za izdelavo zdravila za zdravljenje venske ali arterijske tromboze pri pacientu.
- 15. Uporaba farmacevtsko učinkovite količine spojine po zahtevku 1 ali njene farmacevtsko sprejemljive soli v kombinaciji s heparinom ali heparinom z nizko molekulsko maso za izdelavo zdravila za zdravljenje venske ali arterijske tromboze.
- 16. Uporaba farmacevtsko učinkovite količine spojine po zahtevku 1 ali njene farmacevtsko sprejemljive soli za izdelavo zdravila za zdravljenje restenoze pri pacientu.
- 17. Spojina po zahtevku 11, označena s tem, daje:aliCOOMe ΎΟΟ H2N^-NH ali njena farmacevtsko sprejemljiva sol. AS
- 18. Spojina po zahtevku 11, označena s tem, daje:ali njena farmacevtsko sprejemljiva sol.
- 19. Spojina po zahtevku 11, označena s tem, daje:aliali njena farmacevtsko sprejemljiva sol.
- 20. Spojina po zahtevku 11, označena s tem, daje:ali ali njena farmacevtsko sprejemljiva sol.
- 21. Spojina po zahtevku 11, označena s tem, daje:ali njena farmacevtsko sprejemljiva sol.
- 22. Spojina po zahtevku 11, označena s tem, da je: Oali njena farmacevtsko sprejemljiva sol.
- 23. Spojina po zahtevku 11, označena s tem, daje: 9ali njena farmacevtsko sprejemljiva sol.
- 24. Spojina po zahtevku 11, označena s tem, daje:ali njena farmacevtsko sprejemljiva sol.
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US948596P | 1996-01-02 | 1996-01-02 | |
PCT/US1996/020770 WO1997024118A1 (en) | 1996-01-02 | 1996-12-23 | Substituted n-[(aminoiminomethyl or aminomethyl)phenyl]propyl amides |
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SI9620136A SI9620136A (sl) | 1999-04-30 |
SI9620136B true SI9620136B (en) | 2005-08-31 |
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SI9630629T SI0906094T1 (sl) | 1996-01-02 | 1996-12-23 | Substituirani N-/(aminoiminometil ali aminometil)fenil/propil amidi |
SI9620136A SI9620136B (en) | 1996-01-02 | 1996-12-23 | Substituted n-/(aminoiminomethyl or aminomethyl)phenyl/-propyl amides |
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US (1) | US6140504A (sl) |
EP (1) | EP0906094B1 (sl) |
JP (1) | JP4053597B2 (sl) |
KR (1) | KR100348338B1 (sl) |
CN (1) | CN1273128C (sl) |
AP (1) | AP861A (sl) |
AT (1) | ATE243512T1 (sl) |
AU (1) | AU723338B2 (sl) |
BG (1) | BG64143B1 (sl) |
BR (1) | BR9612423B1 (sl) |
CA (1) | CA2241904C (sl) |
CL (1) | CL2004000376A1 (sl) |
CZ (1) | CZ297544B6 (sl) |
DE (1) | DE69628856T2 (sl) |
DK (1) | DK0906094T3 (sl) |
EA (2) | EA001280B1 (sl) |
ES (1) | ES2197257T3 (sl) |
HK (1) | HK1017613A1 (sl) |
HU (1) | HU228355B1 (sl) |
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PL (1) | PL185460B1 (sl) |
PT (1) | PT906094E (sl) |
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US6080767A (en) * | 1996-01-02 | 2000-06-27 | Aventis Pharmaceuticals Products Inc. | Substituted n-[(aminoiminomethyl or aminomethyl)phenyl]propyl amides |
RO117913B1 (ro) * | 1996-01-02 | 2002-09-30 | Aventis Pharmaceuticals Inc. | Derivaţi de n-[(amino-(imino)metil)fenil]propil amide substituite, compoziţie farmaceutică care îi conţine şi metodă de tratament |
TW542822B (en) | 1997-01-17 | 2003-07-21 | Ajinomoto Kk | Benzamidine derivatives |
BR9814789A (pt) * | 1997-08-26 | 2000-10-10 | Kumiai Chemical Industry Co | Derivados de ácido biarilalquilenocarbamânico e fungicidas agrìcolas e hortìcolas |
US6740682B2 (en) | 1997-08-29 | 2004-05-25 | Tularik Limited | Meta-benzamidine derivatives as serine protease inhibitors |
JP4495339B2 (ja) * | 1998-03-23 | 2010-07-07 | アベンティス・ファーマスーティカルズ・インコーポレイテツド | ピペリジニルおよびn−アミジノピペリジニル誘導体 |
EP1086946A4 (en) * | 1998-06-08 | 2003-03-05 | Ajinomoto Kk | BENZAMIDINE DERIVATIVE |
CA2320730A1 (en) | 1998-12-23 | 2000-07-06 | Renhua Li | Thrombin or factor xa inhibitors |
AU2054700A (en) | 1998-12-23 | 2000-07-31 | Eli Lilly And Company | Antithrombotic amides |
KR20010086461A (ko) | 1998-12-24 | 2001-09-12 | 오흘러 로스 제이. | 인자 xa 억제제로서의 치환된 (아미노이미노메틸 또는아미노메틸)벤조헤테로아릴 화합물 |
EP1022268A1 (en) * | 1999-01-02 | 2000-07-26 | Aventis Pharma Deutschland GmbH | Arylalkanoyl derivatives, processes for their preparation, their use and pharmaceutical compositions containing them |
DE69924527T2 (de) | 1999-01-02 | 2006-02-09 | Sanofi-Aventis Deutschland Gmbh | Arylalkanoylderivate, verfahren zu ihrer herstellung, ihre verwendung und diese enthaltende pharmazeutische zubereitungen |
US6794412B1 (en) * | 1999-03-11 | 2004-09-21 | Bristol-Myers Squibb Pharma Company | Treatment of thrombosis by combined use of a factor Xa inhibitor and aspirin |
DE60022508T2 (de) | 1999-06-14 | 2006-06-08 | Eli Lilly And Co., Indianapolis | Inhibitoren von serin proteasen |
AU776193B2 (en) * | 1999-10-28 | 2004-09-02 | Sankyo Company Limited | Benzamidine derivatives |
CA2389747C (en) | 1999-11-02 | 2011-05-03 | Aventis Pharma Deutschland Gmbh | Use of russell's viper venom-induced plasma factor xa activity to monitor the activity of factor xa inhibitors |
DE10006601A1 (de) | 2000-02-15 | 2001-08-16 | Clariant Gmbh | Verfahren zur Herstellung von 4-(4'-Carboxyphenyl)pyridin |
GB0108903D0 (en) * | 2000-10-05 | 2001-05-30 | Aventis Pharm Prod Inc | Novel crystalline forms of a factor Xa inhibitor |
US7479502B2 (en) | 2002-12-03 | 2009-01-20 | Pharmacyclics, Inc. | 2-(2-hydroxybiphenyl-3-yl)-1H-benzoimidazole-5-carboxamidine derivatives as factor VIIA inhibitors |
DE102006048300A1 (de) * | 2006-01-26 | 2007-08-02 | Hellstern, Peter, Prof. Dr.med. | Inhibitoren des Blutgerinnungsfaktors Xa zur Verwendung als Antikoagulans |
BRPI1011322A2 (pt) * | 2009-04-17 | 2018-09-18 | Merz Pharma Gmbh & Co Kgaa | 1-amino-1,3,3,5,5-pentametilciclohexano mesilato, seu processo de fabricação, suas partículas e seus cristais, uso de anisol ou uma mistura de anisol e pelo menos um dos solventes, e composição farmacêutica. |
RU2542455C2 (ru) | 2009-07-29 | 2015-02-20 | Санофи | Отамиксабан для лечения инфаркта миокарда без подъема сегмента st у пациентов пожилого возраста и пациентов с нарушенной функцией почек |
GB0919194D0 (en) | 2009-11-02 | 2009-12-16 | Lytix Biopharma As | Compounds |
SI2691371T1 (sl) | 2011-03-29 | 2015-07-31 | Sanofi | Sol benzojske kisline otamiksabana |
AU2012234323A1 (en) | 2011-03-29 | 2013-10-17 | Sanofi | Otamixaban formulations with improved stability |
JP6043290B2 (ja) | 2011-09-22 | 2016-12-14 | 武田薬品工業株式会社 | 縮合複素環化合物 |
EA201590473A1 (ru) | 2012-08-31 | 2015-06-30 | Санофи | Отамиксабан для применения в лечении острого коронарного синдрома без подъема st у пациентов, которым планируется проведение аортокоронарного шунтирования |
DE102014108210A1 (de) | 2014-06-11 | 2015-12-17 | Dietrich Gulba | Rodentizid |
US10351750B2 (en) | 2017-02-03 | 2019-07-16 | Saudi Arabian Oil Company | Drilling fluid compositions with enhanced rheology and methods of using same |
EP4070658A1 (de) | 2021-04-06 | 2022-10-12 | BIORoxx GmbH | Verwendung von blutgerinnungshemmenden verbindungen als rodentizide |
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US5424334A (en) * | 1991-12-19 | 1995-06-13 | G. D. Searle & Co. | Peptide mimetic compounds useful as platelet aggregation inhibitors |
RO117913B1 (ro) * | 1996-01-02 | 2002-09-30 | Aventis Pharmaceuticals Inc. | Derivaţi de n-[(amino-(imino)metil)fenil]propil amide substituite, compoziţie farmaceutică care îi conţine şi metodă de tratament |
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