JP2004517920A5 - - Google Patents
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- JP2004517920A5 JP2004517920A5 JP2002559068A JP2002559068A JP2004517920A5 JP 2004517920 A5 JP2004517920 A5 JP 2004517920A5 JP 2002559068 A JP2002559068 A JP 2002559068A JP 2002559068 A JP2002559068 A JP 2002559068A JP 2004517920 A5 JP2004517920 A5 JP 2004517920A5
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- JP
- Japan
- Prior art keywords
- alkyl
- group
- aryl
- formula
- independently
- 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.)
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- 125000000217 alkyl group Chemical group 0.000 claims 123
- 125000003118 aryl group Chemical group 0.000 claims 44
- 150000001875 compounds Chemical class 0.000 claims 40
- 150000003839 salts Chemical class 0.000 claims 40
- 239000011780 sodium chloride Substances 0.000 claims 40
- 239000012453 solvate Substances 0.000 claims 40
- 239000000203 mixture Substances 0.000 claims 25
- 125000003545 alkoxy group Chemical group 0.000 claims 22
- 229910052739 hydrogen Inorganic materials 0.000 claims 20
- 239000003112 inhibitor Substances 0.000 claims 20
- 230000002401 inhibitory effect Effects 0.000 claims 20
- 239000000651 prodrug Substances 0.000 claims 20
- 229940002612 prodrugs Drugs 0.000 claims 20
- 125000001424 substituent group Chemical group 0.000 claims 20
- -1 butyldimethylsilyloxymethyl Chemical group 0.000 claims 18
- 239000001257 hydrogen Substances 0.000 claims 18
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 14
- 125000001072 heteroaryl group Chemical class 0.000 claims 13
- 150000003432 sterols Chemical class 0.000 claims 13
- 235000003702 sterols Nutrition 0.000 claims 13
- 125000005843 halogen group Chemical class 0.000 claims 12
- 125000002947 alkylene group Chemical group 0.000 claims 11
- 238000010521 absorption reaction Methods 0.000 claims 10
- 150000002431 hydrogen Chemical class 0.000 claims 10
- 210000004369 Blood Anatomy 0.000 claims 9
- 239000008280 blood Substances 0.000 claims 9
- UFHFLCQGNIYNRP-UHFFFAOYSA-N hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 8
- 125000001797 benzyl group Chemical class [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])* 0.000 claims 7
- 239000003795 chemical substances by application Substances 0.000 claims 7
- 125000004432 carbon atoms Chemical group C* 0.000 claims 6
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 claims 6
- 125000000753 cycloalkyl group Chemical group 0.000 claims 6
- IJGRMHOSHXDMSA-UHFFFAOYSA-N nitrogen Chemical compound N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims 6
- QTBSBXVTEAMEQO-UHFFFAOYSA-M acetate Chemical compound CC([O-])=O QTBSBXVTEAMEQO-UHFFFAOYSA-M 0.000 claims 5
- 239000003146 anticoagulant agent Substances 0.000 claims 5
- 230000003750 conditioning Effects 0.000 claims 5
- 125000002541 furyl group Chemical group 0.000 claims 5
- 229910052736 halogen Inorganic materials 0.000 claims 5
- 150000002367 halogens Chemical class 0.000 claims 5
- 229920000669 heparin Polymers 0.000 claims 5
- 125000002883 imidazolyl group Chemical group 0.000 claims 5
- 125000003226 pyrazolyl group Chemical group 0.000 claims 5
- 125000004076 pyridyl group Chemical group 0.000 claims 5
- 125000000168 pyrrolyl group Chemical group 0.000 claims 5
- 125000003003 spiro group Chemical group 0.000 claims 5
- 238000006467 substitution reaction Methods 0.000 claims 5
- 125000000335 thiazolyl group Chemical group 0.000 claims 5
- 125000001544 thienyl group Chemical group 0.000 claims 5
- 230000002792 vascular Effects 0.000 claims 5
- HVYWMOMLDIMFJA-DPAQBDIFSA-N (3β)-Cholest-5-en-3-ol Chemical compound C1C=C2C[C@@H](O)CC[C@]2(C)[C@@H]2[C@@H]1[C@@H]1CC[C@H]([C@H](C)CCCC(C)C)[C@@]1(C)CC2 HVYWMOMLDIMFJA-DPAQBDIFSA-N 0.000 claims 4
- OHJKXVLJWUPWQG-IUYNYSEKSA-J (4S,6R)-6-[(2R,4R)-4,6-dihydroxy-5-(sulfonatoamino)-2-(sulfonatooxymethyl)oxan-3-yl]oxy-3,4-dihydroxy-5-sulfonatooxyoxane-2-carboxylate Chemical compound O[C@@H]1C(NS([O-])(=O)=O)C(O)O[C@H](COS([O-])(=O)=O)C1O[C@H]1C(OS([O-])(=O)=O)[C@@H](O)C(O)C(C([O-])=O)O1 OHJKXVLJWUPWQG-IUYNYSEKSA-J 0.000 claims 4
- VEXZGXHMUGYJMC-UHFFFAOYSA-N HCl Chemical compound Cl VEXZGXHMUGYJMC-UHFFFAOYSA-N 0.000 claims 4
- 125000004450 alkenylene group Chemical group 0.000 claims 4
- 125000003282 alkyl amino group Chemical group 0.000 claims 4
- 229910052799 carbon Inorganic materials 0.000 claims 4
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 4
- 125000003387 indolinyl group Chemical group N1(CCC2=CC=CC=C12)* 0.000 claims 4
- 125000000842 isoxazolyl group Chemical group 0.000 claims 4
- 125000002757 morpholinyl group Chemical group 0.000 claims 4
- 229910052757 nitrogen Inorganic materials 0.000 claims 4
- 125000003386 piperidinyl group Chemical group 0.000 claims 4
- 125000000719 pyrrolidinyl group Chemical group 0.000 claims 4
- URSPTJYSBTXILH-UHFFFAOYSA-N 1-methylidenepiperazin-1-ium-4-ide Chemical group C=[N+]1CC[N-]CC1 URSPTJYSBTXILH-UHFFFAOYSA-N 0.000 claims 3
- 206010012601 Diabetes mellitus Diseases 0.000 claims 3
- HTTJABKRGRZYRN-UHFFFAOYSA-N Enoxaparin Chemical compound OC1C(NC(=O)C)C(O)OC(COS(O)(=O)=O)C1OC1C(OS(O)(=O)=O)C(O)C(OC2C(C(OS(O)(=O)=O)C(OC3C(C(O)C(O)C(O3)C(O)=O)OS(O)(=O)=O)C(CO)O2)NS(O)(=O)=O)C(C(O)=O)O1 HTTJABKRGRZYRN-UHFFFAOYSA-N 0.000 claims 3
- 108010054265 Factor VIIa Proteins 0.000 claims 3
- 229940012414 Factor VIIa Drugs 0.000 claims 3
- 108010074860 Factor Xa Proteins 0.000 claims 3
- 229920001499 Heparinoid Polymers 0.000 claims 3
- 208000008589 Obesity Diseases 0.000 claims 3
- 210000002381 Plasma Anatomy 0.000 claims 3
- 102100008880 TFPI Human genes 0.000 claims 3
- 101710034269 TFPI Proteins 0.000 claims 3
- 125000003342 alkenyl group Chemical group 0.000 claims 3
- OKTJSMMVPCPJKN-UHFFFAOYSA-N carbon Chemical compound [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 claims 3
- 125000002993 cycloalkylene group Chemical group 0.000 claims 3
- 239000002554 heparinoid Substances 0.000 claims 3
- 125000000592 heterocycloalkyl group Chemical class 0.000 claims 3
- 239000003607 modifier Substances 0.000 claims 3
- 125000001624 naphthyl group Chemical group 0.000 claims 3
- 235000020824 obesity Nutrition 0.000 claims 3
- 125000002971 oxazolyl group Chemical group 0.000 claims 3
- 125000000951 phenoxy group Chemical group [H]C1=C([H])C([H])=C(O*)C([H])=C1[H] 0.000 claims 3
- 125000000843 phenylene group Chemical group C1(=C(C=CC=C1)*)* 0.000 claims 3
- 239000000106 platelet aggregation inhibitor Substances 0.000 claims 3
- 125000003373 pyrazinyl group Chemical group 0.000 claims 3
- 125000000714 pyrimidinyl group Chemical group 0.000 claims 3
- MNFORVFSTILPAW-UHFFFAOYSA-N Β-Lactam Chemical group O=C1CCN1 MNFORVFSTILPAW-UHFFFAOYSA-N 0.000 claims 3
- CTPOHARTNNSRSR-APJZLKAGSA-N 4-[(1R,2R,3aS,8bS)-2-hydroxy-1-[(E,3S)-3-hydroxy-4-methyloct-1-en-6-ynyl]-2,3,3a,8b-tetrahydro-1H-cyclopenta[b][1]benzofuran-5-yl]butanoic acid Chemical compound O([C@H]1C[C@@H](O)[C@@H]([C@@H]21)/C=C/[C@@H](O)C(C)CC#CC)C1=C2C=CC=C1CCCC(O)=O CTPOHARTNNSRSR-APJZLKAGSA-N 0.000 claims 2
- OIRCOABEOLEUMC-GEJPAHFPSA-N Bivalirudin Chemical compound C([C@@H](C(=O)N[C@@H](CCC(O)=O)C(=O)N[C@@H](CCC(O)=O)C(=O)N[C@@H]([C@@H](C)CC)C(=O)N1[C@@H](CCC1)C(=O)N[C@@H](CCC(O)=O)C(=O)N[C@@H](CCC(O)=O)C(=O)N[C@@H](CC=1C=CC(O)=CC=1)C(=O)N[C@@H](CC(C)C)C(O)=O)NC(=O)[C@H](CC(O)=O)NC(=O)CNC(=O)[C@H](CC(N)=O)NC(=O)CNC(=O)CNC(=O)CNC(=O)CNC(=O)[C@H]1N(CCC1)C(=O)[C@H](CCCNC(N)=N)NC(=O)[C@H]1N(CCC1)C(=O)[C@H](N)CC=1C=CC=CC=1)C1=CC=CC=C1 OIRCOABEOLEUMC-GEJPAHFPSA-N 0.000 claims 2
- 210000001772 Blood Platelets Anatomy 0.000 claims 2
- 229940107161 Cholesterol Drugs 0.000 claims 2
- RRGUKTPIGVIEKM-UHFFFAOYSA-N Cilostazol Chemical compound C=1C=C2NC(=O)CCC2=CC=1OCCCCC1=NN=NN1C1CCCCC1 RRGUKTPIGVIEKM-UHFFFAOYSA-N 0.000 claims 2
- 229940018872 Dalteparin Sodium Drugs 0.000 claims 2
- CGIGDMFJXJATDK-UHFFFAOYSA-N Indometacin Chemical compound CC1=C(CC(O)=O)C2=CC(OC)=CC=C2N1C(=O)C1=CC=C(Cl)C=C1 CGIGDMFJXJATDK-UHFFFAOYSA-N 0.000 claims 2
- 229950002383 Orbofiban Drugs 0.000 claims 2
- QLNJFJADRCOGBJ-UHFFFAOYSA-N Propanamide Chemical compound CCC(N)=O QLNJFJADRCOGBJ-UHFFFAOYSA-N 0.000 claims 2
- 229960001138 acetylsalicylic acid Drugs 0.000 claims 2
- 125000004644 alkyl sulfinyl group Chemical group 0.000 claims 2
- 125000004390 alkyl sulfonyl group Chemical group 0.000 claims 2
- 125000004414 alkyl thio group Chemical group 0.000 claims 2
- 230000002429 anti-coagulation Effects 0.000 claims 2
- 125000004104 aryloxy group Chemical class 0.000 claims 2
- BSYNRYMUTXBXSQ-UHFFFAOYSA-N aspirin Chemical compound CC(=O)OC1=CC=CC=C1C(O)=O BSYNRYMUTXBXSQ-UHFFFAOYSA-N 0.000 claims 2
- IVRMZWNICZWHMI-UHFFFAOYSA-N azide Chemical compound [N-]=[N+]=[N-] IVRMZWNICZWHMI-UHFFFAOYSA-N 0.000 claims 2
- 125000001164 benzothiazolyl group Chemical group S1C(=NC2=C1C=CC=C2)* 0.000 claims 2
- 125000000051 benzyloxy group Chemical class [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])O* 0.000 claims 2
- 229960002890 beraprost Drugs 0.000 claims 2
- 230000037348 biosynthesis Effects 0.000 claims 2
- 230000015572 biosynthetic process Effects 0.000 claims 2
- 229960001500 bivalirudin Drugs 0.000 claims 2
- 108010055460 bivalirudin Proteins 0.000 claims 2
- 235000012000 cholesterol Nutrition 0.000 claims 2
- 229960004588 cilostazol Drugs 0.000 claims 2
- 125000005879 dioxolanyl group Chemical group 0.000 claims 2
- VJDOPFARMOLELX-ZDUSSCGKSA-N ethyl 3-[[(3S)-1-(4-carbamimidoylphenyl)-2-oxopyrrolidin-3-yl]carbamoylamino]propanoate Chemical compound O=C1[C@@H](NC(=O)NCCC(=O)OCC)CCN1C1=CC=C(C(N)=N)C=C1 VJDOPFARMOLELX-ZDUSSCGKSA-N 0.000 claims 2
- 239000002319 fibrinogen receptor antagonist Substances 0.000 claims 2
- 125000003392 indanyl group Chemical group C1(CCC2=CC=CC=C12)* 0.000 claims 2
- 125000003454 indenyl group Chemical group C1(C=CC2=CC=CC=C12)* 0.000 claims 2
- 125000001786 isothiazolyl group Chemical group 0.000 claims 2
- 239000003055 low molecular weight heparin Substances 0.000 claims 2
- 125000004043 oxo group Chemical group O=* 0.000 claims 2
- 239000008194 pharmaceutical composition Substances 0.000 claims 2
- 125000002098 pyridazinyl group Chemical group 0.000 claims 2
- 125000003107 substituted aryl group Chemical group 0.000 claims 2
- 125000001712 tetrahydronaphthyl group Chemical group C1(CCCC2=CC=CC=C12)* 0.000 claims 2
- 230000001225 therapeutic Effects 0.000 claims 2
- 125000001113 thiadiazolyl group Chemical group 0.000 claims 2
- 229960003425 tirofiban Drugs 0.000 claims 2
- COKMIXFXJJXBQG-NRFANRHFSA-N tirofiban Chemical compound C1=CC(C[C@H](NS(=O)(=O)CCCC)C(O)=O)=CC=C1OCCCCC1CCNCC1 COKMIXFXJJXBQG-NRFANRHFSA-N 0.000 claims 2
- GBLQGXFTPLQBTA-UHFFFAOYSA-N 1,2,3-triazoline Chemical class C1CN=NN1 GBLQGXFTPLQBTA-UHFFFAOYSA-N 0.000 claims 1
- RCNHFUDTRRGRGW-UHFFFAOYSA-N 1,2-benzothiazin-4-one Chemical compound C1=CC=C2C(=O)C=NSC2=C1 RCNHFUDTRRGRGW-UHFFFAOYSA-N 0.000 claims 1
- YETULFFXNIHQLK-UHFFFAOYSA-N 1-ethynyl-4-(2-fluorophenyl)benzene Chemical compound FC1=CC=CC=C1C1=CC=C(C#C)C=C1 YETULFFXNIHQLK-UHFFFAOYSA-N 0.000 claims 1
- OICPCODTYMAQOE-UHFFFAOYSA-N 1-phenyl-2,3-dihydropyrrole-5-carboximidamide Chemical compound NC(=N)C1=CCCN1C1=CC=CC=C1 OICPCODTYMAQOE-UHFFFAOYSA-N 0.000 claims 1
- CVJRRJMEMYTWRC-UHFFFAOYSA-N 1-phenylpyrrolidine-2-carboximidamide Chemical compound NC(=N)C1CCCN1C1=CC=CC=C1 CVJRRJMEMYTWRC-UHFFFAOYSA-N 0.000 claims 1
- JKCHHDHEHOKKQP-UHFFFAOYSA-N 1H-imidazol-2-ylboronic acid Chemical compound OB(O)C1=NC=CN1 JKCHHDHEHOKKQP-UHFFFAOYSA-N 0.000 claims 1
- TWWNPUZQYVWXJY-UHFFFAOYSA-N 1H-quinazoline-4-thione Chemical compound C1=CC=C2C(S)=NC=NC2=C1 TWWNPUZQYVWXJY-UHFFFAOYSA-N 0.000 claims 1
- 125000003821 2-(trimethylsilyl)ethoxymethyl group Chemical group [H]C([H])([H])[Si](C([H])([H])[H])(C([H])([H])[H])C([H])([H])C(OC([H])([H])[*])([H])[H] 0.000 claims 1
- ASSKVPFEZFQQNQ-UHFFFAOYSA-N 2-Benzoxazolol Chemical compound C1=CC=C2OC(O)=NC2=C1 ASSKVPFEZFQQNQ-UHFFFAOYSA-N 0.000 claims 1
- BYDKEYCXCIVOOV-JTSKRJEESA-N 2-[[(2S)-4-[[(3S)-1-carbamimidoylpiperidin-3-yl]methylamino]-2-(naphthalen-2-ylsulfonylamino)-4-oxobutanoyl]-cyclopropylamino]acetic acid Chemical compound C1N(C(=N)N)CCC[C@H]1CNC(=O)C[C@@H](C(=O)N(CC(O)=O)C1CC1)NS(=O)(=O)C1=CC=C(C=CC=C2)C2=C1 BYDKEYCXCIVOOV-JTSKRJEESA-N 0.000 claims 1
- ZBLJEMQEPGCCJA-UHFFFAOYSA-N 2-phenyl-1,2-oxazolidine-3-carboximidamide Chemical compound NC(=N)C1CCON1C1=CC=CC=C1 ZBLJEMQEPGCCJA-UHFFFAOYSA-N 0.000 claims 1
- FKMCYKOPRFRZDN-UHFFFAOYSA-N 3,1-benzoxazine-4-thione Chemical compound C1=CC=C2C(=S)OC=NC2=C1 FKMCYKOPRFRZDN-UHFFFAOYSA-N 0.000 claims 1
- HYTIPJFUWHYQON-UHFFFAOYSA-N 3,4-dihydro-1H-quinoxalin-2-one Chemical compound C1=CC=C2NC(=O)CNC2=C1 HYTIPJFUWHYQON-UHFFFAOYSA-N 0.000 claims 1
- BBPRUNPUJIUXSE-DXKRWKNPSA-N 3-[2-[[(1S,2R,3S,4R)-3-[4-(pentylcarbamoyl)-1,3-oxazol-2-yl]-7-oxabicyclo[2.2.1]heptan-2-yl]methyl]phenyl]propanoic acid Chemical compound CCCCCNC(=O)C1=COC([C@H]2[C@H]([C@@H]3CC[C@H]2O3)CC=2C(=CC=CC=2)CCC(O)=O)=N1 BBPRUNPUJIUXSE-DXKRWKNPSA-N 0.000 claims 1
- 101700019104 3SPM Proteins 0.000 claims 1
- 101700016269 3SPT Proteins 0.000 claims 1
- MBGGBVCUIVRRBF-UHFFFAOYSA-N 4-[2-(benzenesulfinyl)ethyl]-1,2-diphenylpyrazolidine-3,5-dione Chemical compound O=C1N(C=2C=CC=CC=2)N(C=2C=CC=CC=2)C(=O)C1CCS(=O)C1=CC=CC=C1 MBGGBVCUIVRRBF-UHFFFAOYSA-N 0.000 claims 1
- PJVWKTKQMONHTI-UHFFFAOYSA-N 4-hydroxy-3-(3-oxo-1-phenylbutyl)-1-benzopyran-2-one Chemical compound OC=1C2=CC=CC=C2OC(=O)C=1C(CC(=O)C)C1=CC=CC=C1 PJVWKTKQMONHTI-UHFFFAOYSA-N 0.000 claims 1
- 229960004676 ANTITHROMBOTIC AGENTS Drugs 0.000 claims 1
- RTRQQBHATOEIAF-UUOKFMHZSA-N Acadesine Chemical group NC1=C(C(=O)N)N=CN1[C@H]1[C@H](O)[C@H](O)[C@@H](CO)O1 RTRQQBHATOEIAF-UUOKFMHZSA-N 0.000 claims 1
- 229960003555 Anagrelide hydrochloride Drugs 0.000 claims 1
- KXNPVXPOPUZYGB-XYVMCAHJSA-N Argatroban Chemical compound OC(=O)[C@H]1C[C@H](C)CCN1C(=O)[C@H](CCCN=C(N)N)NS(=O)(=O)C1=CC=CC2=C1NC[C@H](C)C2 KXNPVXPOPUZYGB-XYVMCAHJSA-N 0.000 claims 1
- MXMZCLLIUQEKSN-UHFFFAOYSA-N Benzimidazoline Chemical compound C1=CC=C2NCNC2=C1 MXMZCLLIUQEKSN-UHFFFAOYSA-N 0.000 claims 1
- NUNZGJKXTJMXGY-UHFFFAOYSA-N C1=CC=C2NC(C(=N)N)=CC2=C1 Chemical compound C1=CC=C2NC(C(=N)N)=CC2=C1 NUNZGJKXTJMXGY-UHFFFAOYSA-N 0.000 claims 1
- 229960003958 Clopidogrel bisulfate Drugs 0.000 claims 1
- 229960004969 Dalteparin Drugs 0.000 claims 1
- 229960004776 Danaparoid sodium Drugs 0.000 claims 1
- DOBMPNYZJYQDGZ-UHFFFAOYSA-N Dicoumarol Chemical compound C1=CC=CC2=C1OC(=O)C(CC=1C(OC3=CC=CC=C3C=1O)=O)=C2O DOBMPNYZJYQDGZ-UHFFFAOYSA-N 0.000 claims 1
- 229960002768 Dipyridamole Drugs 0.000 claims 1
- IZEKFCXSFNUWAM-UHFFFAOYSA-N Dipyridamole Chemical compound C=12N=C(N(CCO)CCO)N=C(N3CCCCC3)C2=NC(N(CCO)CCO)=NC=1N1CCCCC1 IZEKFCXSFNUWAM-UHFFFAOYSA-N 0.000 claims 1
- MBMBGCFOFBJSGT-KUBAVDMBSA-N Docosahexaenoic acid Chemical compound CC\C=C/C\C=C/C\C=C/C\C=C/C\C=C/C\C=C/CCC(O)=O MBMBGCFOFBJSGT-KUBAVDMBSA-N 0.000 claims 1
- OEHFRZLKGRKFAS-UHFFFAOYSA-N Droxicam Chemical compound C12=CC=CC=C2S(=O)(=O)N(C)C(C2=O)=C1OC(=O)N2C1=CC=CC=N1 OEHFRZLKGRKFAS-UHFFFAOYSA-N 0.000 claims 1
- 229960000610 Enoxaparin Drugs 0.000 claims 1
- 229960005153 Enoxaparin sodium Drugs 0.000 claims 1
- 229960003013 Epoprostenol Sodium Drugs 0.000 claims 1
- 229950003750 FLURETOFEN Drugs 0.000 claims 1
- ZFGMDIBRIDKWMY-PASTXAENSA-N Heparin Chemical compound CC(O)=N[C@@H]1[C@@H](O)[C@H](O)[C@@H](COS(O)(=O)=O)O[C@@H]1O[C@@H]1[C@@H](C(O)=O)O[C@@H](O[C@H]2[C@@H]([C@@H](OS(O)(=O)=O)[C@@H](O[C@@H]3[C@@H](OC(O)[C@H](OS(O)(=O)=O)[C@H]3O)C(O)=O)O[C@@H]2O)CS(O)(=O)=O)[C@H](O)[C@H]1O ZFGMDIBRIDKWMY-PASTXAENSA-N 0.000 claims 1
- 229960001008 Heparin sodium Drugs 0.000 claims 1
- 229940025770 Heparinoids Drugs 0.000 claims 1
- 241000257303 Hymenoptera Species 0.000 claims 1
- HEFNNWSXXWATRW-UHFFFAOYSA-N Ibuprofen Chemical compound CC(C)CC1=CC=C(C(C)C(O)=O)C=C1 HEFNNWSXXWATRW-UHFFFAOYSA-N 0.000 claims 1
- 229950004274 Ifetroban Drugs 0.000 claims 1
- 229960000905 Indomethacin Drugs 0.000 claims 1
- 102000000853 LDL receptors Human genes 0.000 claims 1
- 108010001831 LDL receptors Proteins 0.000 claims 1
- 102000004895 Lipoproteins Human genes 0.000 claims 1
- 108090001030 Lipoproteins Proteins 0.000 claims 1
- 229940103185 Mefenamate Drugs 0.000 claims 1
- HYYBABOKPJLUIN-UHFFFAOYSA-N Mefenamic acid Chemical compound CC1=CC=CC(NC=2C(=CC=CC=2)C(O)=O)=C1C HYYBABOKPJLUIN-UHFFFAOYSA-N 0.000 claims 1
- BXJUYPRTOQQTSS-UHFFFAOYSA-N N-[1-[[3-(aminomethyl)phenyl]methyl]-5-oxopyrrolidin-3-yl]dibenzofuran-2-sulfonamide Chemical compound NCC1=CC=CC(CN2C(CC(C2)NS(=O)(=O)C=2C=C3C4=CC=CC=C4OC3=CC=2)=O)=C1 BXJUYPRTOQQTSS-UHFFFAOYSA-N 0.000 claims 1
- 150000001204 N-oxides Chemical class 0.000 claims 1
- FSUPKDUNLKQBCN-UHFFFAOYSA-N NC(=N)C1=CC=CN1 Chemical compound NC(=N)C1=CC=CN1 FSUPKDUNLKQBCN-UHFFFAOYSA-N 0.000 claims 1
- LEZHMTGJGJTOBP-FQEVSTJZSA-N NN=CC=1C=C(CN2C([C@H](CC2)NS(=O)(=O)N2CC3=CC=CC=C3CC2)=O)C=CC1 Chemical compound NN=CC=1C=C(CN2C([C@H](CC2)NS(=O)(=O)N2CC3=CC=CC=C3CC2)=O)C=CC1 LEZHMTGJGJTOBP-FQEVSTJZSA-N 0.000 claims 1
- MQQNFDZXWVTQEH-UHFFFAOYSA-N Nafamostat Chemical compound C1=CC(N=C(N)N)=CC=C1C(=O)OC1=CC=C(C=C(C=C2)C(N)=N)C2=C1 MQQNFDZXWVTQEH-UHFFFAOYSA-N 0.000 claims 1
- CMWTZPSULFXXJA-VIFPVBQESA-N Naproxen Chemical compound C1=C([C@H](C)C(O)=O)C=CC2=CC(OC)=CC=C21 CMWTZPSULFXXJA-VIFPVBQESA-N 0.000 claims 1
- 229950005835 Napsagatran Drugs 0.000 claims 1
- JOXIMZWYDAKGHI-UHFFFAOYSA-N P-Toluenesulfonic acid Chemical compound CC1=CC=C(S(O)(=O)=O)C=C1 JOXIMZWYDAKGHI-UHFFFAOYSA-N 0.000 claims 1
- BYPFEZZEUUWMEJ-UHFFFAOYSA-N Pentoxifylline Chemical compound O=C1N(CCCCC(=O)C)C(=O)N(C)C2=C1N(C)C=N2 BYPFEZZEUUWMEJ-UHFFFAOYSA-N 0.000 claims 1
- 229960001476 Pentoxifylline Drugs 0.000 claims 1
- QYSPLQLAKJAUJT-UHFFFAOYSA-N Piroxicam Chemical compound OC=1C2=CC=CC=C2S(=O)(=O)N(C)C=1C(=O)NC1=CC=CC=N1 QYSPLQLAKJAUJT-UHFFFAOYSA-N 0.000 claims 1
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-
2002
- 2002-01-25 RU RU2003126185/15A patent/RU2314126C2/ru not_active IP Right Cessation
- 2002-01-25 WO PCT/US2002/002013 patent/WO2002058734A2/en active IP Right Grant
- 2002-01-25 HU HU0303917A patent/HUP0303917A2/hu unknown
- 2002-01-25 IL IL15648802A patent/IL156488A0/xx unknown
- 2002-01-25 JP JP2002559068A patent/JP2004517920A/ja active Pending
- 2002-01-25 EP EP02704233A patent/EP1353694B1/en not_active Expired - Lifetime
- 2002-01-25 DK DK02704233T patent/DK1353694T3/da active
- 2002-01-25 KR KR10-2003-7009794A patent/KR20040025890A/ko not_active Application Discontinuation
- 2002-01-25 AR ARP020100271A patent/AR032403A1/es not_active Application Discontinuation
- 2002-01-25 BR BR0206639-4A patent/BR0206639A/pt not_active IP Right Cessation
- 2002-01-25 SI SI200230652T patent/SI1353694T1/sl unknown
- 2002-01-25 CA CA002434504A patent/CA2434504A1/en not_active Abandoned
- 2002-01-25 PL PL02364178A patent/PL364178A1/xx not_active Application Discontinuation
- 2002-01-25 CN CN028042204A patent/CN1658903A/zh active Pending
- 2002-01-25 PT PT02704233T patent/PT1353694E/pt unknown
- 2002-01-25 ES ES02704233T patent/ES2296894T3/es not_active Expired - Lifetime
- 2002-01-25 KR KR1020087015928A patent/KR20080067717A/ko not_active Application Discontinuation
- 2002-01-25 US US10/056,680 patent/US20020147184A1/en not_active Abandoned
- 2002-01-25 CZ CZ20032039A patent/CZ20032039A3/cs unknown
- 2002-01-25 EP EP07009475A patent/EP1810693A3/en not_active Withdrawn
- 2002-01-25 MX MXPA03006728A patent/MXPA03006728A/es active IP Right Grant
- 2002-01-25 SK SK950-2003A patent/SK9502003A3/sk not_active Application Discontinuation
- 2002-01-25 AU AU2002237927A patent/AU2002237927B2/en not_active Ceased
- 2002-01-25 DE DE60224163T patent/DE60224163T2/de not_active Expired - Fee Related
- 2002-01-25 AT AT02704233T patent/ATE381347T1/de not_active IP Right Cessation
- 2002-01-25 NZ NZ542090A patent/NZ542090A/en unknown
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2003
- 2003-07-25 NO NO20033357A patent/NO20033357L/no not_active Application Discontinuation
- 2003-12-17 HK HK03109198A patent/HK1056695A1/xx not_active IP Right Cessation
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