FI120494B - Faktor Xa inhibitorer - Google Patents
Faktor Xa inhibitorer Download PDFInfo
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- FI120494B FI120494B FI964317A FI964317A FI120494B FI 120494 B FI120494 B FI 120494B FI 964317 A FI964317 A FI 964317A FI 964317 A FI964317 A FI 964317A FI 120494 B FI120494 B FI 120494B
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- chg
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- paph
- leu
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- C07K14/8107—Endopeptidase (E.C. 3.4.21-99) inhibitors
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- C07K5/06—Dipeptides
- C07K5/06008—Dipeptides with the first amino acid being neutral
- C07K5/06017—Dipeptides with the first amino acid being neutral and aliphatic
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- C07K5/06—Dipeptides
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- C07K5/0804—Tripeptides with the first amino acid being neutral and aliphatic
- C07K5/0806—Tripeptides with the first amino acid being neutral and aliphatic the side chain containing 0 or 1 carbon atoms, i.e. Gly, Ala
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- C07K5/08—Tripeptides
- C07K5/0802—Tripeptides with the first amino acid being neutral
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- C07K5/08—Tripeptides
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- C07K5/08—Tripeptides
- C07K5/0821—Tripeptides with the first amino acid being heterocyclic, e.g. His, Pro, Trp
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- C07K5/10—Tetrapeptides
- C07K5/1002—Tetrapeptides with the first amino acid being neutral
- C07K5/1005—Tetrapeptides with the first amino acid being neutral and aliphatic
- C07K5/101—Tetrapeptides with the first amino acid being neutral and aliphatic the side chain containing 2 to 4 carbon atoms, e.g. Val, Ile, Leu
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- C07K5/10—Tetrapeptides
- C07K5/1002—Tetrapeptides with the first amino acid being neutral
- C07K5/1016—Tetrapeptides with the first amino acid being neutral and aromatic or cycloaliphatic
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- C—CHEMISTRY; METALLURGY
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- C07K7/64—Cyclic peptides containing only normal peptide links
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- C12Q1/00—Measuring or testing processes involving enzymes, nucleic acids or microorganisms; Compositions therefor; Processes of preparing such compositions
- C12Q1/56—Measuring or testing processes involving enzymes, nucleic acids or microorganisms; Compositions therefor; Processes of preparing such compositions involving blood clotting factors, e.g. involving thrombin, thromboplastin, fibrinogen
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K38/00—Medicinal preparations containing peptides
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- Y—GENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
- Y02—TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
- Y02P—CLIMATE CHANGE MITIGATION TECHNOLOGIES IN THE PRODUCTION OR PROCESSING OF GOODS
- Y02P20/00—Technologies relating to chemical industry
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- Y02P20/55—Design of synthesis routes, e.g. reducing the use of auxiliary or protecting groups
Claims (18)
1. Förening, som inhiberar specifikt faktor Xa -aktivitet och som har den allmänna formeln 5 Xi-R1-R2-R3-X2 varvid Xl är H, en acyl-, alkyl- eller arylalkylgrupp;
2. Förening, som inhiberar specifikt faktor Xa - • · • "·· aktivitet och som har den allmänna formeln • · Γ·*: A1-A2-A3-B • · .:. 25 • · · · . .·. varvid • · · AI är Tyr, F(pNH2), mAph, pAph, eller Nal(2), som innehal- • · · ler 0 eller 1 aminoskyddsgrupper; ... A2 är Ile eller Chg; • · ·
30 A3 är Arg, PalMe(3), Dab (Νγ-03Η7Ν) , Dap (Np-C3H7N) eller Orn (Νδ03Η7Ν) ; och B är -H, -OH, -NH2, 1-5 aminosyror eller en karboxyls- :*“. kyddsgrupp, inkluderande farmaceutiskt godtagbara salter ··· av förningen. • · · *^* 35
3. Förening enligt patentkrav 1 eller 2, varvid aminos- • · '.··' kyddsgruppen väljs ur en grupp, som utgörs av formyl, ace- 82 tyl, pikoloyl, tert-butylacetyl, tert-butyloxikarbonyl, bensyloxikarbonyl, 2-aryl-2-0-bensyloxim, aminoacyl, bensoyl, tosyl, 3-fenoxipropion, 5-bensimidazolkarboxi, CC1F2-C0, CF2H-CO, CF3-CF2CO, CH3-CHCl-CO, CH3-0-C0, ch3-so2, ch3ch2-o-co, 5 Cl2CHCO, CIH2CO, (pOH)C6H4-CH2CH(OH)-CO, (pOH) C6H4-CH2CHOH- CO, (pOH) C6H4-OCH (CH3) CO, (pOH) C6H4-OCH2CO, 4-MeO-C6H4-CO, N-morfolinyl-CO, Ph-C (NOCH2Ph)-CO, Ph-CH=CH-CO, Ph-CH2CH2CH2-CO, Ph-CH2CH2-CO, trifluoroacetyl, eller är en substituent i den N-terminala aminogruppen, vilken substituent är en 10 cyklopentylkarboxyl-, isokinolylkarboxyl- tai pyrazinkar- boxylgrupp.
4. Förening enligt patentkraven 1-3, varvid det farmaceutiskt godtagbara saltet är ett syraadditionssalt.
5 Ac-Nal(2)-Chg-Arg-Leu-Pro-NH2, Ac~pAph-Chg-PalMe-NH2, Ac-D-pAph-Chg-Pal(Me)-Leu-Pro-NH2, Ac-D-pAph-Chg-Pal(Me)-NH2, och Ac-Phe (pNH2) -Chg-Arg-Leu-Pro-NH2.
5 Ac-pAph-Chg-PalMe(3)-L-P-NH2; Ac-pAph-Chg-R-NH2 ; Ac-pAph-Chg-R-OH; DIPA-(m)pAph-Chg-R-L-P-NH2; DIPA- (m) F(pNH2) -Chg-R-L-P-NH2;
5 Ac-(iBu)Phe(pNH2)-Chg-Arg-NH2; Ac-pAph-Chg-Arg-NH2 ; CF3C(0) - (iBu) Phe (pNH2) -Chg-Arg-NH2; Ac-pAph-Chg-Arg-NH2; Ac-pAph-Chg-Pal(3)Me-NH2;
5. Förening enligt patentkrav 4, varvid syraaddi-15 tionssaltet är ett salt, som bildas av en oorganisk syra, som väljs ur en grupp, som utgörs av klorvätesyra, bromvä-tesyra, svavelsyra, eller perklorsyra, eller är ett sait, som bildas av en organisk syra, som väljs ur en grupp, som utgörs av ättiksyra, oxalsyra, maleinsyra, malinsyra, vin-20 syra, citronsyra, bärnstensyra eller malonsyra.
6. Förening enligt patentkraven 1-5, varvid det • · : *·· farmaceutiskt godtagbara saltet väljs ur en grupp, som ut- *:·*: görs av oorganiskt nitrat, sulfat, acetat, malat, formiat, ·*·": laktat, tartrat, succinat, citrat och p-toluensulfonat. • · •j. 25
7. Förening enligt patentkrav 6, varvid det farma- • ·· · . ceutskt godtagbara saltet är p-toluensulfonat. • · ·
8. Förening enligt patentkraven 1 och 3-7, var- • · · vid Xl väljs ur en grupp, som utgörs av metyl, etyl, n-pro- ... pyi, isopropyl, sek-butyl, 1-metylbutyl, 2,2-dimetylbutyl, • · · 30 2-metylpentyl, 2,2-dimetylpropyl, n-pentyl, n-hexyl, cyk- ’···* lopentyl, metyl-cyklohexyl och cyklopropyl-metyleeni, for- myi, acetyl, bensoyl, bensyl, pikolyl. •
9. Förening enligt patentkraven 1 och 3-7, var- • · · vid den orala estern väljs ur en grupp, som utgörs av ai- • · · *·*·* 35 koximetylgrupper, a- (C3.-C4) alkoxietylgrupper, 2-oxo-l, 3-dio- • · xolen-4-ylmetylgrupper, Ci-C3~alkyltiometylgrupper, acyloxime- 83 tylgrupper, α-acyloxi-a-substituerade metylgrupper, 1-(Οχ-C/j-alkyloxikarbonyloxi)et-l-ylgrupper och 1-(Ci-CU-alkylia-minokarbonyloxi)et-l-ylgrupper.
10 Isn-F(pNH2)-Chg-R-L-P-NH2; Pza-F (pNH2) -Chg-R-L-P-NH2; Tfa-(iBu)Y-Chg-R-L-P-NH2; Tfa- (iBu) Y-l-Orn (N5-C3H7N) -L-P-NH2; Ac-pAph-Chg-PalMe(3)-NH-CH2"Chx;
10 CF3C(0) (iBu)-Tyr-Ile-Arg-NH2; Ac-pAph-Chg-PalMe(3)-NH-CH2-Chx; Ac-pAph-Chg-PalMe(3)-NH-2CMT; Ac-pAph-Chg-PalMe(3)-NH-Chx; Ac-F(pNH2) -Chg-Dab (Νγ-03ΝΗ7) -L-P-NH2;
10. Förening enligt patentkrav 9, varvid den orala 5 estern väljs ur en grupp, sora utgörs av metoxiraetyl, eto- ximetyl, iso-propoximetyl, metoxietyl, etoxietyl, propoxi-etyl, isoproxietyl, 5-metyl-2-oxo-l,3-dioxolen-4-ylmetyl, 5-fenyl-2-oxo-l,3-dioxolen-4-ylmetyl, metyltiometyl, etyl-tiometyl, isopropyltioraetyl, pivaloyloximetyl, a-acetoxi-10 metyl, etoxikarbonyl-l-metyl, α-acetoxietyl, 3-ftalidyl, 5, 6-dimetylftalidyl, 1-etoxsikarbonylox)et-l-yl och l-(me-tylaminokarbonyloxi)et-l-yl.
10 Rl är Tyr; R2 är Ile; R3 är Arg; och X2 väljs ur en grupp, som utgörs av en modifierad C-ter-minalgrupp, en eller flera karboxylskyddsgrupper, en eller 15 flera aminosyror eller annan substituent, varvid den modi-fierade C-terminalgruppen är modifierad genom att reducera den C-terminala karboxylgruppen till en alkohol eller al-dehyd eller genom att bilda en oral ester eller genom att substituera karboxylgruppen med en substituent; inklude-20 rande farmaceutiskt godtagbsra salter av föreningen.
11. Förening enligt patentkraven 1-10, som väljs ur en grupp, sora utgörs av
12. Farmaceutisk komposition innehällande en fö- rening enligt nägot av patentkraven 1-11.
13. Farmaceutisk komposition enligt patentkrav 11 innehällande ytterligare en farmaceutiskt godtagbar bära-re.
14. Användning av en förening enligt nägot av pa tentkraven 1-11 vid framställning av en farmaceutisk komposition för specifik inhibering av aktiviteten hos faktorn Xa.
15. Användning enligt patentkrav 14, varvid den 20 farmaceutiska kompositionen är avsedd för behandling av kardiovaskulära sjukdomar, som väljs ur en grupp, som ut- • · • ’·· görs av restenos efter angioplastik, andningsbesvärsyndrom *ί**ί hos fullvuxen, bristande f lerorgansfunktion, stroke och :*·*: disseminerad intravaskulär koagulation-levringsstörning. ··· 25
16. Användning enligt patentkrav 14, varvid den ···· . .·. farmaceutiska kompositionen är avsedd för behandling av störningar som hänför sig till kirurgi, som väljs ur en • · « grupp, som utgörs av djupven- eller proximal ventrombos.
... 17. Användning enligt patentkrav 14, varvid den • · · 30 farmaceutiska kompositionen är avsedd att reducera eller • · *···* inhibera blodlevring.
15 Ac-pAph-Chg-PalMe(3)-NH-Chx; Bzf-pAph-Chg-PalMe(3)-NH2; Ac-pAph-Chg-PalMe(3)-L-P-NH2; Ac-pAph-Chg-PalMe(3)-NH2; cyklopentyl-CO-pAph-Chg-PalMe(3)-NH2; 20 3-lqc-pAph-Chg-PalMe{3)-NH2; 2-furoyl-pAph-Chg-PalMe (3) -NH2; • *·· 5-Me-tienyl-CO-pAph~Chg-PalMe(3)-NH2; ·:**: Ac-pAph-Chg-PalMe (3) -ol; ·'·*; Ac-Tyr~Ile~Arg-Leu-Ala-NH2, • · .:. 25 Ac-Tyr-Ile-Arg-Leu-Pro-NH2/ . .·. Ac- (iBu) Tyr-Ile-Arg-Leu-Pro-NH2, • · · Ac-Tyr-Ile-Arg-N (CH3) 0 (CH3} , Ac-Tyr{Ψ(CH2NH) }-Ile-Arg~Leu-Pro-NH2, Ac-Tyr~Ile-Arg-NH-CH2(4-pyridyl) , : 30 Ac-Tyr-lie {Ψ (CH2NH) } -Arg-Leu-Pro-NH2, :...: Ac-Tyr-Chg-Arg (N02) - {Ψ (CH2NH) }-Leu-NH2, Ac-Tyr-lle-Arg-{¥(COCH2) }-Gly-Pro-NH2, .*·*. Ac-Tyr-Ile-Dab (Ny-C3H7N) -Leu-Ala-NH2, Ac-Tyr-Ile-PalMe(3)-NH2, *·*·* 35 Tyr-Ile-Arg-NH2, ··· *...' D-Tyr-Ile-Arg-Leu-Pro-NH2/ 86 Ac-(Bzl)Gly-(Chx)Gly-(3-guanidopropyl)Gly-NH2, cyklo(Gly-Tyr-Ile-Arg-Gly) , Tfa-(iBu)Tyr-Chg-Arg-Leu-Pro-NH2, Ac-pAph-Chg-Arg-Leu-Pro-NH2,
15 Bz-F(pNH2)-Chg-R-L-P-NH2; Tos-F(pNH2) -Chg-R-L-P-NH2; Ac-Y(3-1)-Chg-R-L-P-NH2; y-Chg-R-L-NH2; Ac-F(pNH2) -Chg-R-ol; 20 cyklopentyl-CO-pAph-Chg-PalMe(3)-NH2; 3-lqc-pAph-Chg-PalMe(3)-NH2; !*··. Bzi-pAph-Chg-PalMe (3) -NH2; *:**: 3-lqc-F (pNH2) -Chg-R-L-P-NH2; ·*·’: Ac-F (pNH2) -Chg-R-NH-2-tiazolyl; • · ··. 25 2-furoyl-pAph-Chg-PalMe (3)-NH2; . .·. 5-Me-2-tienyl-CO-pAph-Chg-PalMe (3)-NH2; Ac-Nal (2) -Chg-R-NH-2-tiazolyl; ’ * 2-Bzf-F (pNH2) -Chg-R-L-P-NH2; Äc-pAph-Chg-Dab (NY-C3H7N) -L-P-NH2; • · ·
30 Ac- (iBu)pAph-Chg-R-L-P-NH2; Ac-pAph-Chg-R-Gla-P-NH2; Ac-pAph-Chg-R-Pen (CH2COOH) -P-NH2; .***. Ac-pAph-Chg-R-L-P-NH2; Ac-F (pNH2) -Chg-R- (Me)L~P-NH2; • · · *;]·’ 35 Ac-F (pNH2) -Chg-R-OEt; :···: Ac-F (pNH2) -Chg-Orn (N5-C3H7N) -L-P-NH2; 85 Ac-F (pNH2) -Chg-R-L-P-NH2; Ac-Nal(2)-Chg-R-L-P-NH2; Ac-pAph-Chg-Dab (NY-C3H7N) -NH2; Ac-pAph-Chg-PalMe(3)-NH2;
15 CF3C (O) -(iBu) Phe (NH2) -Chg-Arg-Leu-Pro-NH2; Ac-pAph-Ile-Arg-Leu-Pro-NH2; CF3C(0)-(iBu)Nal(2)-Chg~Arg-Leu-Pro-NH2; Ac-Phe(31,4NH2)-Chg-Arg-Leu-Pro-NH2; CF3C(0)-Tyr-Chg-Arg-Leu-Pro-NH2; 20 (5-bensimidazoyl) -Phe (NH2) -Chg-Arg-Leu-Pro-NH2; CF3C(0)-(iBu)Tyr-Ile-Arg-Leu-Pro-NH2; • *·· Ac- (Chx-CH2) Tyr-Ile-Arg-Leu~Pro-NH2; *:*·: D-Tyr-Chg-Arg-Leu-Pro-NH2; :*·*: Ac-Trp-Chg-Arg-Leu~Pro-NH2; • · .:. 25 Ac-pAph-Chg-Arg-Leu-Pro-NH2; • · · · . .·. Ac-pAgh-Chg-Arg-Gla-Pro-NH2; ,···. Ac- (iBu)Nal (2) -Chg-Arg-Leu-Pro-NH2; • · · Ac-Phe(p-C0NH2) -Chg-Arg-Leu-Pro-NH2; ... Ac-pAph-Ile-Arg-Leu-Pro-NH2; • « ·
30 Ac-Phe (pNH2)-Chg-Arg-(Me) Leu-Pro-NH2; Ac- (Chx-CH2) Tyr-Chg-Arg-Leu-Pro-NH2; Ac-pAph-Chg-Pal (3)Me-Leu-Pro-NH2; (bensoyl) -Phe (pNH2) Chg-Arg-Leu-Pro-NH2; • · # .*. Ac- (2-raetylpentanyl) -Tyr-Ile-Arg-Leu-Pro-NH2; • · ·
35 Ac-(2-metylbutyl) Tyr-Ile~Arg“Leu-Pro-NH2; ’···* Ac-Phe (pNH2) -Chg-Arg-Leu-Pro-NH2; 84 Ac-Tyr-Chg-Ärg-Leu-Pro-NH2; Ac-(iBu)-Phe(pNH2)-Chg-Arg-Leu-Pro-NH2; Ac-(Chx-CH2) -Tyr-Ile-Arg-Leu-Pro-NH2; (2-bensofuroyl)-pAph-Chg-Pal(3)Me-NH2;
18. Användning av en förening enligt nägot av pa- :1: tentkraven 1-11 som antikoagulant för inhibering av ··· .*. blodprovskoagulation. • · · • · · • · • · • · ···
Applications Claiming Priority (4)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US23305494A | 1994-04-26 | 1994-04-26 | |
US23305494 | 1994-04-26 | ||
US9505268 | 1995-04-25 | ||
PCT/US1995/005268 WO1995029189A1 (en) | 1994-04-26 | 1995-04-25 | FACTOR Xa INHIBITORS |
Publications (3)
Publication Number | Publication Date |
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FI964317A0 FI964317A0 (sv) | 1996-10-25 |
FI964317A FI964317A (sv) | 1996-10-25 |
FI120494B true FI120494B (sv) | 2009-11-13 |
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ID=22875692
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Application Number | Title | Priority Date | Filing Date |
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FI964317A FI120494B (sv) | 1994-04-26 | 1996-10-25 | Faktor Xa inhibitorer |
Country Status (27)
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EP (2) | EP0758341B1 (sv) |
JP (1) | JP3655632B2 (sv) |
KR (1) | KR100380124B1 (sv) |
CN (1) | CN1181091C (sv) |
AT (1) | ATE262536T1 (sv) |
AU (1) | AU707653B2 (sv) |
CA (1) | CA2186497C (sv) |
CZ (1) | CZ296439B6 (sv) |
DE (1) | DE69532754T2 (sv) |
DK (1) | DK0758341T3 (sv) |
EE (1) | EE03973B1 (sv) |
ES (1) | ES2214500T3 (sv) |
FI (1) | FI120494B (sv) |
HU (1) | HUT76346A (sv) |
IL (1) | IL113505A (sv) |
LT (1) | LT4218B (sv) |
LV (1) | LV11740B (sv) |
NO (1) | NO318759B1 (sv) |
NZ (1) | NZ284977A (sv) |
PL (1) | PL188132B1 (sv) |
PT (1) | PT758341E (sv) |
RU (1) | RU2152954C1 (sv) |
SI (1) | SI9520044B (sv) |
SK (1) | SK286094B6 (sv) |
TW (1) | TW409129B (sv) |
WO (1) | WO1995029189A1 (sv) |
ZA (1) | ZA953361B (sv) |
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EP1016663A1 (en) * | 1999-01-02 | 2000-07-05 | Aventis Pharma Deutschland GmbH | Novel malonic acid derivatives, processes for their preparation, their use and pharmaceutical compositions containing them (inhibition of factor Xa activity) |
BR9916732A (pt) * | 1999-01-02 | 2001-09-25 | Aventis Pharma Gmbh | Derivados de ácido malÈnico, processo para a sua preparação, seu uso e composições farmacêuticas contendo-os (inibição da atividade do fator xa) |
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EP1095933A1 (en) | 1999-10-30 | 2001-05-02 | Aventis Pharma Deutschland GmbH | Novel N-guanidinoalkylamides, their preparation, their use, and pharmaceutical preparations comprising them |
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JP5088598B2 (ja) * | 1999-12-14 | 2012-12-05 | 昭和電工株式会社 | シアノベンジルアミン類の塩の製造方法 |
RU2250212C2 (ru) * | 2000-01-28 | 2005-04-20 | Авентис Фарма Дойчланд Гмбх | Способ получения ацетиламидиниофенилаланилциклогексилглицилпиридиниоаланинамидов |
EP1127884A1 (en) * | 2000-02-26 | 2001-08-29 | Aventis Pharma Deutschland GmbH | Novel malonic acid derivatives, processes for their preparation, their use as inhibitor of factor XA activity and pharmaceutical compositions containing them |
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EP1314733A1 (en) | 2001-11-22 | 2003-05-28 | Aventis Pharma Deutschland GmbH | Indole-2-carboxamides as factor Xa inhibitors |
DE50310038D1 (de) | 2002-03-11 | 2008-08-07 | Curacyte Ag | Hemmstoffe der urokinase, ihre herstellung und verwendung |
PT1569912E (pt) | 2002-12-03 | 2015-09-15 | Pharmacyclics Llc | Derivados 2-(2-hidroxibifenil-3-il)-1h-benzoimidazole-5- carboxamidina como inibidores do fator viia |
US7358268B2 (en) | 2002-12-04 | 2008-04-15 | Sanofi-Aventis Deutschland Gmbh | Imidazole derivatives as factor Xa inhibitors |
US7429581B2 (en) | 2002-12-23 | 2008-09-30 | Sanofi-Aventis Deutschland Gmbh | Pyrazole-derivatives as factor Xa inhibitors |
DE10301300B4 (de) | 2003-01-15 | 2009-07-16 | Curacyte Chemistry Gmbh | Verwendung von acylierten 4-Amidino- und 4-Guanidinobenzylaminen zur Inhibierung von Plasmakallikrein |
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EP1479677A1 (en) | 2003-05-19 | 2004-11-24 | Aventis Pharma Deutschland GmbH | New indole derivatives as factor xa inhibitors |
EP1479680A1 (en) | 2003-05-19 | 2004-11-24 | Aventis Pharma Deutschland GmbH | Azaindole derivatives as Factor Xa inhibitors |
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EP1479675A1 (en) | 2003-05-19 | 2004-11-24 | Aventis Pharma Deutschland GmbH | Indazole-derivatives as factor Xa inhibitors |
US7741341B2 (en) | 2003-05-19 | 2010-06-22 | Sanofi-Aventis Deutschland Gmbh | Benzimidazole-derivatives as factor Xa inhibitors |
DE10342108A1 (de) | 2003-09-11 | 2005-04-14 | Curacyte Chemistry Gmbh | Basisch-substituierte Benzylaminanaloga als Inhibitoren des Gerinnungsfaktors Xa, ihre Herstellung und Verwendung |
EP1568698A1 (en) | 2004-02-27 | 2005-08-31 | Aventis Pharma Deutschland GmbH | Pyrrole-derivatives as factor Xa inhibitors |
US7446210B2 (en) | 2004-10-26 | 2008-11-04 | Janssen Pharmaceutica N.V. | Factor Xa compounds |
EP1724269A1 (en) | 2005-05-20 | 2006-11-22 | Sanofi-Aventis Deutschland GmbH | Heteroaryl-carboxylic acid (sulfamoyl alkyl) amide - derivatives as factor Xa inhibitors |
DE102005044319A1 (de) | 2005-09-16 | 2007-03-22 | Curacyte Chemistry Gmbh | 2-(Aminomethyl)-5-Chlor-Benzylamid-Derivate und ihre Verwendung als Hemmstoffe des Gerinnungsfaktors Xa |
DE102006050672A1 (de) | 2006-10-24 | 2008-04-30 | Curacyte Discovery Gmbh | Hemmstoffe des Plasmins und des Plasmakallikreins |
EP1918718A1 (de) * | 2006-10-31 | 2008-05-07 | Roche Diagnostics GmbH | Verfahren und Vorrichtungen zur elektrochemischen Bestimmung von Faktor Xa-Inhibitoren in Blutproben |
EP2591783A1 (en) | 2007-04-13 | 2013-05-15 | Millennium Pharmaceuticals, Inc. | Combination anticoagulant therapy with a compound that acts as a factor Xa inhibitor |
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US4275153A (en) * | 1978-08-03 | 1981-06-23 | American Hospital Supply Corporation | Analytical fluorogenic substrates for proteolytic enzymes |
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US4469679A (en) * | 1983-02-16 | 1984-09-04 | Smithkline Beckman Corporation | Octapeptide vasopressin antagonists |
HU191961B (en) * | 1984-08-02 | 1987-04-28 | Richter Gedeon Vegyeszet | Process for producing 1,5 and 8 substituted peptides of angiotenzin-ii antagonistic activity |
DE69321344D1 (de) * | 1992-02-14 | 1998-11-05 | Corvas Int Inc | Inhibitoren der thrombose |
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1995
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- 1995-04-25 HU HU9602954A patent/HUT76346A/hu not_active Application Discontinuation
- 1995-04-25 WO PCT/US1995/005268 patent/WO1995029189A1/en active IP Right Grant
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- 1995-04-25 DE DE69532754T patent/DE69532754T2/de not_active Expired - Lifetime
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- 1995-04-25 EP EP03021617A patent/EP1384725A3/en not_active Withdrawn
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- 1995-04-25 PT PT95917736T patent/PT758341E/pt unknown
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- 1995-04-26 IL IL11350595A patent/IL113505A/xx not_active IP Right Cessation
- 1995-05-11 TW TW084104681A patent/TW409129B/zh active
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- 1996-10-25 FI FI964317A patent/FI120494B/sv not_active IP Right Cessation
- 1996-10-25 NO NO19964553A patent/NO318759B1/no not_active IP Right Cessation
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