JP2004513888A - アミノ複素環式化合物（第Ｘａ因子阻害剤１４） - Google Patents
アミノ複素環式化合物（第Ｘａ因子阻害剤１４） Download PDFInfo
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- JP2004513888A JP2004513888A JP2002529067A JP2002529067A JP2004513888A JP 2004513888 A JP2004513888 A JP 2004513888A JP 2002529067 A JP2002529067 A JP 2002529067A JP 2002529067 A JP2002529067 A JP 2002529067A JP 2004513888 A JP2004513888 A JP 2004513888A
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- JP
- Japan
- Prior art keywords
- yloxy
- aminoisoquinolin
- amide
- methanesulfonylbiphenyl
- pentanoic acid
- 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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- -1 Amino heterocyclic compounds Chemical class 0.000 title claims description 16
- 229940123583 Factor Xa inhibitor Drugs 0.000 title 1
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- 239000003814 drug Substances 0.000 claims abstract description 5
- 238000004519 manufacturing process Methods 0.000 claims abstract description 5
- 150000003839 salts Chemical class 0.000 claims description 12
- 108010014173 Factor X Proteins 0.000 claims description 8
- WLHWAZBTXBASEZ-UHFFFAOYSA-N 2-(1-aminoisoquinolin-7-yl)oxy-n-[4-(2-methylsulfonylphenyl)phenyl]pentanamide Chemical compound C=1C=C2C=CN=C(N)C2=CC=1OC(CCC)C(=O)NC(C=C1)=CC=C1C1=CC=CC=C1S(C)(=O)=O WLHWAZBTXBASEZ-UHFFFAOYSA-N 0.000 claims description 6
- 208000007536 Thrombosis Diseases 0.000 claims description 6
- 239000003112 inhibitor Substances 0.000 claims description 5
- 229910052757 nitrogen Inorganic materials 0.000 claims description 5
- 125000001624 naphthyl group Chemical group 0.000 claims description 4
- 125000004430 oxygen atom Chemical group O* 0.000 claims description 4
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims description 4
- 239000012453 solvate Substances 0.000 claims description 4
- 125000004434 sulfur atom Chemical group 0.000 claims description 4
- ZQGCHSOSHUJKSS-UHFFFAOYSA-N 2-(1-aminoisoquinolin-7-yl)oxy-n-[4-(3-cyanophenyl)phenyl]pentanamide Chemical compound C=1C=C2C=CN=C(N)C2=CC=1OC(CCC)C(=O)NC(C=C1)=CC=C1C1=CC=CC(C#N)=C1 ZQGCHSOSHUJKSS-UHFFFAOYSA-N 0.000 claims description 3
- 206010002383 Angina Pectoris Diseases 0.000 claims description 3
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- 206010022562 Intermittent claudication Diseases 0.000 claims description 3
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- 208000010125 myocardial infarction Diseases 0.000 claims description 3
- 208000037803 restenosis Diseases 0.000 claims description 3
- FLXQZJOYBMXKAQ-UHFFFAOYSA-N 2-(1-aminoisoquinolin-5-yl)oxy-n-[4-(2-methylsulfonylphenyl)phenyl]hexanamide Chemical compound C=1C=CC2=C(N)N=CC=C2C=1OC(CCCC)C(=O)NC(C=C1)=CC=C1C1=CC=CC=C1S(C)(=O)=O FLXQZJOYBMXKAQ-UHFFFAOYSA-N 0.000 claims description 2
- INZDTXRWESPHGV-UHFFFAOYSA-N 2-(1-aminoisoquinolin-5-yl)oxy-n-[4-(2-methylsulfonylphenyl)phenyl]pentanamide Chemical compound C=1C=CC2=C(N)N=CC=C2C=1OC(CCC)C(=O)NC(C=C1)=CC=C1C1=CC=CC=C1S(C)(=O)=O INZDTXRWESPHGV-UHFFFAOYSA-N 0.000 claims description 2
- FCNRUISBKQCYRQ-UHFFFAOYSA-N 2-(1-aminoisoquinolin-5-yl)oxy-n-[4-(2-sulfamoylphenyl)phenyl]hexanamide Chemical compound C=1C=CC2=C(N)N=CC=C2C=1OC(CCCC)C(=O)NC(C=C1)=CC=C1C1=CC=CC=C1S(N)(=O)=O FCNRUISBKQCYRQ-UHFFFAOYSA-N 0.000 claims description 2
- YWJHYKRQJDXVAL-UHFFFAOYSA-N 2-(1-aminoisoquinolin-5-yl)oxy-n-[4-(2-sulfamoylphenyl)phenyl]pentanamide Chemical compound C=1C=CC2=C(N)N=CC=C2C=1OC(CCC)C(=O)NC(C=C1)=CC=C1C1=CC=CC=C1S(N)(=O)=O YWJHYKRQJDXVAL-UHFFFAOYSA-N 0.000 claims description 2
- UAQYBNIJGWDPSD-UHFFFAOYSA-N 2-(1-aminoisoquinolin-7-yl)oxy-4-methyl-n-[4-(2-methylsulfonylphenyl)phenyl]pentanamide Chemical compound C=1C=C2C=CN=C(N)C2=CC=1OC(CC(C)C)C(=O)NC(C=C1)=CC=C1C1=CC=CC=C1S(C)(=O)=O UAQYBNIJGWDPSD-UHFFFAOYSA-N 0.000 claims description 2
- QQPCLFWXCMQKMZ-UHFFFAOYSA-N 2-(1-aminoisoquinolin-7-yl)oxy-n-[4-(2-cyanophenyl)phenyl]pentanamide Chemical compound C=1C=C2C=CN=C(N)C2=CC=1OC(CCC)C(=O)NC(C=C1)=CC=C1C1=CC=CC=C1C#N QQPCLFWXCMQKMZ-UHFFFAOYSA-N 0.000 claims description 2
- LBJYFDODIYCXGL-UHFFFAOYSA-N 2-(1-aminoisoquinolin-7-yl)oxy-n-[4-(2-ethylsulfonylphenyl)phenyl]pentanamide Chemical compound C=1C=C2C=CN=C(N)C2=CC=1OC(CCC)C(=O)NC(C=C1)=CC=C1C1=CC=CC=C1S(=O)(=O)CC LBJYFDODIYCXGL-UHFFFAOYSA-N 0.000 claims description 2
- HPFKUXOKXNJQPT-UHFFFAOYSA-N 2-(1-aminoisoquinolin-7-yl)oxy-n-[4-(2-methoxyphenyl)phenyl]pentanamide Chemical compound C=1C=C2C=CN=C(N)C2=CC=1OC(CCC)C(=O)NC(C=C1)=CC=C1C1=CC=CC=C1OC HPFKUXOKXNJQPT-UHFFFAOYSA-N 0.000 claims description 2
- FRVUJFZNPSLIBO-UHFFFAOYSA-N 2-(1-aminoisoquinolin-7-yl)oxy-n-[4-(2-methylsulfonylphenyl)phenyl]-2-phenylacetamide Chemical compound CS(=O)(=O)C1=CC=CC=C1C(C=C1)=CC=C1NC(=O)C(C=1C=CC=CC=1)OC1=CC=C(C=CN=C2N)C2=C1 FRVUJFZNPSLIBO-UHFFFAOYSA-N 0.000 claims description 2
- RFNQNXAOJUDJKU-UHFFFAOYSA-N 2-(1-aminoisoquinolin-7-yl)oxy-n-[4-(2-methylsulfonylphenyl)phenyl]hexanamide Chemical compound C=1C=C2C=CN=C(N)C2=CC=1OC(CCCC)C(=O)NC(C=C1)=CC=C1C1=CC=CC=C1S(C)(=O)=O RFNQNXAOJUDJKU-UHFFFAOYSA-N 0.000 claims description 2
- LIKMQWLUFQOTJW-UHFFFAOYSA-N 2-(1-aminoisoquinolin-7-yl)oxy-n-[4-(2-sulfamoylphenyl)phenyl]pentanamide Chemical compound C=1C=C2C=CN=C(N)C2=CC=1OC(CCC)C(=O)NC(C=C1)=CC=C1C1=CC=CC=C1S(N)(=O)=O LIKMQWLUFQOTJW-UHFFFAOYSA-N 0.000 claims description 2
- IYSOBGCWNZESSJ-UHFFFAOYSA-N 2-(1-aminoisoquinolin-7-yl)oxy-n-[[2-(2-methylsulfonylphenyl)phenyl]methyl]pentanamide Chemical compound C=1C=C2C=CN=C(N)C2=CC=1OC(CCC)C(=O)NCC1=CC=CC=C1C1=CC=CC=C1S(C)(=O)=O IYSOBGCWNZESSJ-UHFFFAOYSA-N 0.000 claims description 2
- LACZAVZERFPPKC-UHFFFAOYSA-N 2-(1-aminoisoquinolin-7-yl)oxy-n-[[4-(2-methylsulfonylphenyl)phenyl]methyl]pentanamide Chemical compound C=1C=C2C=CN=C(N)C2=CC=1OC(CCC)C(=O)NCC(C=C1)=CC=C1C1=CC=CC=C1S(C)(=O)=O LACZAVZERFPPKC-UHFFFAOYSA-N 0.000 claims description 2
- VOFQHXRQAPVIAY-UHFFFAOYSA-N 2-(2-aminoquinolin-7-yl)oxy-n-[4-(2-methylsulfonylphenyl)phenyl]pentanamide Chemical compound C=1C=C2C=CC(N)=NC2=CC=1OC(CCC)C(=O)NC(C=C1)=CC=C1C1=CC=CC=C1S(C)(=O)=O VOFQHXRQAPVIAY-UHFFFAOYSA-N 0.000 claims description 2
- GEXKCGKPYGRHCF-UHFFFAOYSA-N 2-[(1-aminoisoquinolin-7-yl)amino]-n-[4-(2-methylsulfonylphenyl)phenyl]-3-phenylpropanamide Chemical compound CS(=O)(=O)C1=CC=CC=C1C(C=C1)=CC=C1NC(=O)C(NC=1C=C2C(N)=NC=CC2=CC=1)CC1=CC=CC=C1 GEXKCGKPYGRHCF-UHFFFAOYSA-N 0.000 claims description 2
- CURLTUGMZLYLDI-UHFFFAOYSA-N Carbon dioxide Chemical group O=C=O CURLTUGMZLYLDI-UHFFFAOYSA-N 0.000 claims description 2
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- CERQOIWHTDAKMF-UHFFFAOYSA-M Methacrylate Chemical compound CC(=C)C([O-])=O CERQOIWHTDAKMF-UHFFFAOYSA-M 0.000 description 1
- 108091005804 Peptidases Proteins 0.000 description 1
- 102000035195 Peptidases Human genes 0.000 description 1
- 239000004264 Petrolatum Substances 0.000 description 1
- 108010094028 Prothrombin Proteins 0.000 description 1
- 102100027378 Prothrombin Human genes 0.000 description 1
- VYPSYNLAJGMNEJ-UHFFFAOYSA-N Silicium dioxide Chemical group O=[Si]=O VYPSYNLAJGMNEJ-UHFFFAOYSA-N 0.000 description 1
- UIIMBOGNXHQVGW-UHFFFAOYSA-M Sodium bicarbonate Chemical class [Na+].OC([O-])=O UIIMBOGNXHQVGW-UHFFFAOYSA-M 0.000 description 1
- 229920002472 Starch Polymers 0.000 description 1
- 108010000499 Thromboplastin Proteins 0.000 description 1
- 102000002262 Thromboplastin Human genes 0.000 description 1
- NNLVGZFZQQXQNW-ADJNRHBOSA-N [(2r,3r,4s,5r,6s)-4,5-diacetyloxy-3-[(2s,3r,4s,5r,6r)-3,4,5-triacetyloxy-6-(acetyloxymethyl)oxan-2-yl]oxy-6-[(2r,3r,4s,5r,6s)-4,5,6-triacetyloxy-2-(acetyloxymethyl)oxan-3-yl]oxyoxan-2-yl]methyl acetate Chemical compound O([C@@H]1O[C@@H]([C@H]([C@H](OC(C)=O)[C@H]1OC(C)=O)O[C@H]1[C@@H]([C@@H](OC(C)=O)[C@H](OC(C)=O)[C@@H](COC(C)=O)O1)OC(C)=O)COC(=O)C)[C@@H]1[C@@H](COC(C)=O)O[C@@H](OC(C)=O)[C@H](OC(C)=O)[C@H]1OC(C)=O NNLVGZFZQQXQNW-ADJNRHBOSA-N 0.000 description 1
- 230000000996 additive effect Effects 0.000 description 1
- 230000002776 aggregation Effects 0.000 description 1
- 238000004220 aggregation Methods 0.000 description 1
- 150000001408 amides Chemical class 0.000 description 1
- 150000001412 amines Chemical group 0.000 description 1
- 230000033115 angiogenesis Effects 0.000 description 1
- 239000007864 aqueous solution Substances 0.000 description 1
- 230000000740 bleeding effect Effects 0.000 description 1
- 239000003114 blood coagulation factor Substances 0.000 description 1
- 229940019700 blood coagulation factors Drugs 0.000 description 1
- 210000004204 blood vessel Anatomy 0.000 description 1
- 230000037396 body weight Effects 0.000 description 1
- 239000000872 buffer Substances 0.000 description 1
- FJDQFPXHSGXQBY-UHFFFAOYSA-L caesium carbonate Chemical compound [Cs+].[Cs+].[O-]C([O-])=O FJDQFPXHSGXQBY-UHFFFAOYSA-L 0.000 description 1
- 229910000024 caesium carbonate Inorganic materials 0.000 description 1
- 239000002775 capsule Substances 0.000 description 1
- 125000000837 carbohydrate group Chemical group 0.000 description 1
- 150000001720 carbohydrates Chemical class 0.000 description 1
- 150000001733 carboxylic acid esters Chemical group 0.000 description 1
- 230000003197 catalytic effect Effects 0.000 description 1
- 238000006555 catalytic reaction Methods 0.000 description 1
- 230000008859 change Effects 0.000 description 1
- 238000003776 cleavage reaction Methods 0.000 description 1
- 239000003086 colorant Substances 0.000 description 1
- 239000006071 cream Substances 0.000 description 1
- 238000004132 cross linking Methods 0.000 description 1
- 239000002552 dosage form Substances 0.000 description 1
- 230000008030 elimination Effects 0.000 description 1
- 238000003379 elimination reaction Methods 0.000 description 1
- 239000003995 emulsifying agent Substances 0.000 description 1
- 239000000839 emulsion Substances 0.000 description 1
- 230000002255 enzymatic effect Effects 0.000 description 1
- 229940088598 enzyme Drugs 0.000 description 1
- 229940012413 factor vii Drugs 0.000 description 1
- 229960000301 factor viii Drugs 0.000 description 1
- 239000000835 fiber Substances 0.000 description 1
- 239000000706 filtrate Substances 0.000 description 1
- 235000013305 food Nutrition 0.000 description 1
- 235000011389 fruit/vegetable juice Nutrition 0.000 description 1
- 239000008273 gelatin Substances 0.000 description 1
- 229920000159 gelatin Polymers 0.000 description 1
- 235000019322 gelatine Nutrition 0.000 description 1
- 235000011852 gelatine desserts Nutrition 0.000 description 1
- ZDXPYRJPNDTMRX-UHFFFAOYSA-N glutamine Natural products OC(=O)C(N)CCC(N)=O ZDXPYRJPNDTMRX-UHFFFAOYSA-N 0.000 description 1
- 239000008187 granular material Substances 0.000 description 1
- 230000036541 health Effects 0.000 description 1
- 150000004677 hydrates Chemical class 0.000 description 1
- 239000007943 implant Substances 0.000 description 1
- 238000001727 in vivo Methods 0.000 description 1
- 238000010348 incorporation Methods 0.000 description 1
- 230000002401 inhibitory effect Effects 0.000 description 1
- DRGUQIQEUWFBDE-UHFFFAOYSA-N isoquinolin-7-amine Chemical compound C1=CN=CC2=CC(N)=CC=C21 DRGUQIQEUWFBDE-UHFFFAOYSA-N 0.000 description 1
- PUIYPHIFMLGHFX-UHFFFAOYSA-N isoquinoline-1,7-diamine Chemical class C1=CN=C(N)C2=CC(N)=CC=C21 PUIYPHIFMLGHFX-UHFFFAOYSA-N 0.000 description 1
- 239000008101 lactose Substances 0.000 description 1
- 239000000314 lubricant Substances 0.000 description 1
- 235000019359 magnesium stearate Nutrition 0.000 description 1
- 230000007246 mechanism Effects 0.000 description 1
- IHCHOVVAJBADAH-UHFFFAOYSA-N n-[2-hydroxy-4-(1h-pyrazol-4-yl)phenyl]-6-methoxy-3,4-dihydro-2h-chromene-3-carboxamide Chemical compound C1C2=CC(OC)=CC=C2OCC1C(=O)NC(C(=C1)O)=CC=C1C=1C=NNC=1 IHCHOVVAJBADAH-UHFFFAOYSA-N 0.000 description 1
- 239000002674 ointment Substances 0.000 description 1
- 239000012074 organic phase Substances 0.000 description 1
- 230000003204 osmotic effect Effects 0.000 description 1
- 230000001590 oxidative effect Effects 0.000 description 1
- 238000007911 parenteral administration Methods 0.000 description 1
- 235000019271 petrolatum Nutrition 0.000 description 1
- 229940066842 petrolatum Drugs 0.000 description 1
- 239000008194 pharmaceutical composition Substances 0.000 description 1
- 230000000144 pharmacologic effect Effects 0.000 description 1
- 239000006187 pill Substances 0.000 description 1
- 229920001223 polyethylene glycol Polymers 0.000 description 1
- 229920000642 polymer Polymers 0.000 description 1
- 230000002980 postoperative effect Effects 0.000 description 1
- 238000002360 preparation method Methods 0.000 description 1
- 239000003755 preservative agent Substances 0.000 description 1
- 125000006239 protecting group Chemical group 0.000 description 1
- 229940039716 prothrombin Drugs 0.000 description 1
- 230000004044 response Effects 0.000 description 1
- ITDJKCJYYAQMRO-UHFFFAOYSA-L rhodium(2+);diacetate Chemical compound [Rh+2].CC([O-])=O.CC([O-])=O ITDJKCJYYAQMRO-UHFFFAOYSA-L 0.000 description 1
- 230000007017 scission Effects 0.000 description 1
- 238000000926 separation method Methods 0.000 description 1
- 239000003001 serine protease inhibitor Substances 0.000 description 1
- 239000000741 silica gel Chemical group 0.000 description 1
- 229910002027 silica gel Chemical group 0.000 description 1
- 230000002269 spontaneous effect Effects 0.000 description 1
- 239000003381 stabilizer Substances 0.000 description 1
- 239000008107 starch Substances 0.000 description 1
- 235000019698 starch Nutrition 0.000 description 1
- 239000000829 suppository Substances 0.000 description 1
- 230000001629 suppression Effects 0.000 description 1
- 239000000725 suspension Substances 0.000 description 1
- 239000006188 syrup Substances 0.000 description 1
- 235000020357 syrup Nutrition 0.000 description 1
- 239000000454 talc Substances 0.000 description 1
- 235000012222 talc Nutrition 0.000 description 1
- 229910052623 talc Inorganic materials 0.000 description 1
- HPRPAQRZFMQZLM-UHFFFAOYSA-N tert-butyl 2-bromopentanoate Chemical compound CCCC(Br)C(=O)OC(C)(C)C HPRPAQRZFMQZLM-UHFFFAOYSA-N 0.000 description 1
- 238000002560 therapeutic procedure Methods 0.000 description 1
- 230000002537 thrombolytic effect Effects 0.000 description 1
- 238000007056 transamidation reaction Methods 0.000 description 1
- 230000008733 trauma Effects 0.000 description 1
- 125000004044 trifluoroacetyl group Chemical group FC(C(=O)*)(F)F 0.000 description 1
- 235000015112 vegetable and seed oil Nutrition 0.000 description 1
- 239000008158 vegetable oil Substances 0.000 description 1
- 229940088594 vitamin Drugs 0.000 description 1
- 239000011782 vitamin Substances 0.000 description 1
- 229930003231 vitamin Natural products 0.000 description 1
- 235000013343 vitamin Nutrition 0.000 description 1
- 239000000080 wetting agent Substances 0.000 description 1
- 230000034365 zymogen activation Effects 0.000 description 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D215/00—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
- C07D215/02—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom
- C07D215/16—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom 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
- C07D215/38—Nitrogen atoms
-
- 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]
-
- 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
-
- 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
-
- 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
- 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D215/00—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
- C07D215/02—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom
- C07D215/16—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom 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
- C07D215/48—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D217/00—Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems
- C07D217/22—Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems 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 carbon atoms of the nitrogen-containing ring
Landscapes
- Chemical & Material Sciences (AREA)
- Health & Medical Sciences (AREA)
- Organic Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Pharmacology & Pharmacy (AREA)
- Engineering & Computer Science (AREA)
- Animal Behavior & Ethology (AREA)
- Public Health (AREA)
- Heart & Thoracic Surgery (AREA)
- Cardiology (AREA)
- Urology & Nephrology (AREA)
- Vascular Medicine (AREA)
- Diabetes (AREA)
- Hematology (AREA)
- Pain & Pain Management (AREA)
- Rheumatology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Other In-Based Heterocyclic Compounds (AREA)
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| DE10046272A DE10046272A1 (de) | 2000-09-19 | 2000-09-19 | Aminoheterocyclen (Faktor Xa Inhibitoren 14) |
| PCT/EP2001/010786 WO2002024654A1 (de) | 2000-09-19 | 2001-09-18 | AMINOHETEROCYCLEN (FAKTOR Xa INHIBITOREN 14) |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| JP2004513888A true JP2004513888A (ja) | 2004-05-13 |
Family
ID=7656743
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2002529067A Pending JP2004513888A (ja) | 2000-09-19 | 2001-09-18 | アミノ複素環式化合物（第Ｘａ因子阻害剤１４） |
Country Status (5)
| Country | Link |
|---|---|
| EP (1) | EP1322618A1 (de) |
| JP (1) | JP2004513888A (de) |
| CA (1) | CA2422067A1 (de) |
| DE (1) | DE10046272A1 (de) |
| WO (1) | WO2002024654A1 (de) |
Families Citing this family (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US6906192B2 (en) | 2000-11-07 | 2005-06-14 | Bristol Myers Squibb Company | Processes for the preparation of acid derivatives useful as serine protease inhibitors |
| EP1332131A2 (de) | 2000-11-07 | 2003-08-06 | Bristol-Myers Squibb Company | Säurederivate und ihre verwendung als inhibitoren von serinproteasen |
| US7030141B2 (en) | 2001-11-29 | 2006-04-18 | Christopher Franklin Bigge | Inhibitors of factor Xa and other serine proteases involved in the coagulation cascade |
| JP2006517589A (ja) * | 2003-02-11 | 2006-07-27 | ブリストル−マイヤーズ スクイブ カンパニー | セリンプロテアーゼ・インヒビターとして有用なベンゼンアセトアミド化合物 |
| US7858666B2 (en) | 2007-06-08 | 2010-12-28 | Mannkind Corporation | IRE-1α inhibitors |
| WO2010117084A1 (en) * | 2009-04-10 | 2010-10-14 | Banyu Pharmaceutical Co.,Ltd. | Novel isoquinoline derivatives |
Family Cites Families (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DE69830410T2 (de) * | 1997-08-29 | 2006-01-26 | Tularik Ltd. | Meta-benzamidinderivate als serinprotease-inhibitoren |
| TW575567B (en) * | 1998-10-23 | 2004-02-11 | Akzo Nobel Nv | Serine protease inhibitor |
| WO2000071508A2 (en) * | 1999-05-24 | 2000-11-30 | Cor Therapeutics, Inc. | INHIBITORS OF FACTOR Xa |
| JP2003500382A (ja) * | 1999-05-24 | 2003-01-07 | シーオーアール セラピューティクス インコーポレイテッド | Ｘａ因子の阻害剤 |
| CA2382751A1 (en) * | 1999-05-24 | 2000-11-30 | Cor Therapeutics, Inc. | Inhibitors of factor xa |
| US20030065176A1 (en) * | 2000-01-29 | 2003-04-03 | Myung-Gyun Kang | Factor xa inhibitors with aryl-amidines and derivatives, and prodrugs thereof |
-
2000
- 2000-09-19 DE DE10046272A patent/DE10046272A1/de not_active Withdrawn
-
2001
- 2001-09-18 JP JP2002529067A patent/JP2004513888A/ja active Pending
- 2001-09-18 CA CA002422067A patent/CA2422067A1/en not_active Abandoned
- 2001-09-18 WO PCT/EP2001/010786 patent/WO2002024654A1/de not_active Application Discontinuation
- 2001-09-18 EP EP01985251A patent/EP1322618A1/de not_active Withdrawn
Also Published As
| Publication number | Publication date |
|---|---|
| CA2422067A1 (en) | 2003-03-12 |
| EP1322618A1 (de) | 2003-07-02 |
| DE10046272A1 (de) | 2002-03-28 |
| WO2002024654A1 (de) | 2002-03-28 |
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