NO319816B1 - Nitrogenholdige heterocykler,anvendelse av disse for fremstilling av medikamenter samt farmasoytiske preparater. - Google Patents

Nitrogenholdige heterocykler,anvendelse av disse for fremstilling av medikamenter samt farmasoytiske preparater. Download PDF

Info

Publication number: NO319816B1
Authority: NO; Norway
Prior art keywords: biphen; methyl; methoxyphenyl; phenyl; aminobenzisoxazol
Prior art date: 1998-12-23

Application number

NO20013072A

Other languages

English (en)

Norwegian (no)

Other versions

NO20013072D0 (no

NO20013072L (no

Inventor

Patrick Yuk-Sun Lam

James Russell Pruitt

Donald Joseph-Phillip Pinto

Joseph Cacciola

John Matthew Fevig

Qi Han

Mimi Lifen Quan

Karen Anita Rossi

Charles G Clark

Original Assignee

Du Pont Pharm Co

Priority date (The priority date 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 date listed.)

1998-12-23

Filing date

2001-06-20

Publication date

2005-09-19

Family has litigation

First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=26811284&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=NO319816(B1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.

2001-06-20 Application filed by Du Pont Pharm Co filed Critical Du Pont Pharm Co

2001-06-20 Publication of NO20013072D0 publication Critical patent/NO20013072D0/no

2001-06-20 Publication of NO20013072L publication Critical patent/NO20013072L/no

2005-09-19 Publication of NO319816B1 publication Critical patent/NO319816B1/no

Links

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229940079593 drug Drugs 0.000 title claims description 8
239000000825 pharmaceutical preparation Substances 0.000 title claims description 6
238000004519 manufacturing process Methods 0.000 title description 6
150000001875 compounds Chemical class 0.000 claims description 381
125000004172 4-methoxyphenyl group Chemical group [H]C1=C([H])C(OC([H])([H])[H])=C([H])C([H])=C1* 0.000 claims description 200
-1 2-(aminosulfonyl)phenyl Chemical group 0.000 claims description 94
125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims description 77
RWRDLPDLKQPQOW-UHFFFAOYSA-N tetrahydropyrrole Natural products C1CCNC1 RWRDLPDLKQPQOW-UHFFFAOYSA-N 0.000 claims description 43
150000003839 salts Chemical class 0.000 claims description 35
229910052757 nitrogen Inorganic materials 0.000 claims description 25
125000000217 alkyl group Chemical group 0.000 claims description 24
125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims description 23
125000000719 pyrrolidinyl group Chemical group 0.000 claims description 23
125000004429 atom Chemical group 0.000 claims description 18
208000001435 Thromboembolism Diseases 0.000 claims description 10
229910052799 carbon Inorganic materials 0.000 claims description 10
125000004169 (C1-C6) alkyl group Chemical group 0.000 claims description 9
125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims description 9
125000004202 aminomethyl group Chemical group [H]N([H])C([H])([H])* 0.000 claims description 8
229910052736 halogen Inorganic materials 0.000 claims description 8
150000002367 halogens Chemical class 0.000 claims description 8
229910052739 hydrogen Inorganic materials 0.000 claims description 8
125000002962 imidazol-1-yl group Chemical group [*]N1C([H])=NC([H])=C1[H] 0.000 claims description 8
RAXXELZNTBOGNW-UHFFFAOYSA-N imidazole Natural products C1=CNC=N1 RAXXELZNTBOGNW-UHFFFAOYSA-N 0.000 claims description 8
125000002883 imidazolyl group Chemical group 0.000 claims description 8
238000002360 preparation method Methods 0.000 claims description 8
125000004198 2-fluorophenyl group Chemical group [H]C1=C([H])C(F)=C(*)C([H])=C1[H] 0.000 claims description 7
239000003937 drug carrier Substances 0.000 claims description 7
125000004523 tetrazol-1-yl group Chemical group N1(N=NN=C1)* 0.000 claims description 7
125000002837 carbocyclic group Chemical group 0.000 claims description 6
125000001995 cyclobutyl group Chemical group [H]C1([H])C([H])([H])C([H])(*)C1([H])[H] 0.000 claims description 6
125000001511 cyclopentyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])(*)C1([H])[H] 0.000 claims description 6
125000004433 nitrogen atom Chemical group N* 0.000 claims description 6
125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 claims description 6
ZYHQGITXIJDDKC-UHFFFAOYSA-N 2-[2-(2-aminophenyl)ethyl]aniline Chemical group NC1=CC=CC=C1CCC1=CC=CC=C1N ZYHQGITXIJDDKC-UHFFFAOYSA-N 0.000 claims description 4
125000004180 3-fluorophenyl group Chemical group [H]C1=C([H])C(*)=C([H])C(F)=C1[H] 0.000 claims description 4
125000004186 cyclopropylmethyl group Chemical group [H]C([H])(*)C1([H])C([H])([H])C1([H])[H] 0.000 claims description 4
125000003261 o-tolyl group Chemical group [H]C1=C([H])C(*)=C(C([H])=C1[H])C([H])([H])[H] 0.000 claims description 4
125000004076 pyridyl group Chemical group 0.000 claims description 4
238000002560 therapeutic procedure Methods 0.000 claims description 4
125000004182 2-chlorophenyl group Chemical group [H]C1=C([H])C(Cl)=C(*)C([H])=C1[H] 0.000 claims description 3
125000004179 3-chlorophenyl group Chemical group [H]C1=C([H])C(*)=C([H])C(Cl)=C1[H] 0.000 claims description 3
125000006615 aromatic heterocyclic group Chemical group 0.000 claims description 3
125000003386 piperidinyl group Chemical group 0.000 claims description 3
125000003831 tetrazolyl group Chemical group 0.000 claims description 3
XZMVYWXGZUMIFK-UHFFFAOYSA-N 1,4,5,6-tetrahydropyrazolo[3,4-c]pyridin-7-one Chemical compound O=C1NCCC2=C1NN=C2 XZMVYWXGZUMIFK-UHFFFAOYSA-N 0.000 claims description 2
125000002947 alkylene group Chemical group 0.000 claims description 2
125000001797 benzyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])* 0.000 claims description 2
125000005047 dihydroimidazolyl group Chemical group N1(CNC=C1)* 0.000 claims description 2
QJGQUHMNIGDVPM-UHFFFAOYSA-N nitrogen group Chemical group [N] QJGQUHMNIGDVPM-UHFFFAOYSA-N 0.000 claims description 2
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TVEXGJYMHHTVKP-UHFFFAOYSA-N 6-oxabicyclo[3.2.1]oct-3-en-7-one Chemical compound C1C2C(=O)OC1C=CC2 TVEXGJYMHHTVKP-UHFFFAOYSA-N 0.000 claims 1
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125000001207 fluorophenyl group Chemical group 0.000 claims 1
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239000000243 solution Substances 0.000 description 286
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239000011541 reaction mixture Substances 0.000 description 159
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239000000203 mixture Substances 0.000 description 142
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239000012267 brine Substances 0.000 description 116
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239000003039 volatile agent Substances 0.000 description 112
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238000005481 NMR spectroscopy Methods 0.000 description 75
238000000034 method Methods 0.000 description 71
239000000741 silica gel Substances 0.000 description 71
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WYURNTSHIVDZCO-UHFFFAOYSA-N Tetrahydrofuran Chemical group C1CCOC1 WYURNTSHIVDZCO-UHFFFAOYSA-N 0.000 description 69
230000002829 reductive effect Effects 0.000 description 61
238000003756 stirring Methods 0.000 description 60
238000000746 purification Methods 0.000 description 58
230000002441 reversible effect Effects 0.000 description 58
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BWHMMNNQKKPAPP-UHFFFAOYSA-L potassium carbonate Chemical compound [K+].[K+].[O-]C([O-])=O BWHMMNNQKKPAPP-UHFFFAOYSA-L 0.000 description 36
VHYFNPMBLIVWCW-UHFFFAOYSA-N 4-Dimethylaminopyridine Chemical compound CN(C)C1=CC=NC=C1 VHYFNPMBLIVWCW-UHFFFAOYSA-N 0.000 description 34
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NFHFRUOZVGFOOS-UHFFFAOYSA-N palladium;triphenylphosphane Chemical compound [Pd].C1=CC=CC=C1P(C=1C=CC=CC=1)C1=CC=CC=C1.C1=CC=CC=C1P(C=1C=CC=CC=1)C1=CC=CC=C1.C1=CC=CC=C1P(C=1C=CC=CC=1)C1=CC=CC=C1.C1=CC=CC=C1P(C=1C=CC=CC=1)C1=CC=CC=C1 NFHFRUOZVGFOOS-UHFFFAOYSA-N 0.000 description 34
238000002953 preparative HPLC Methods 0.000 description 34
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238000006243 chemical reaction Methods 0.000 description 29
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239000008024 pharmaceutical diluent Substances 0.000 description 1
239000000546 pharmaceutical excipient Substances 0.000 description 1
230000003285 pharmacodynamic effect Effects 0.000 description 1
125000004934 phenanthridinyl group Chemical group C1(=CC=CC2=NC=C3C=CC=CC3=C12)* 0.000 description 1
125000001791 phenazinyl group Chemical group C1(=CC=CC2=NC3=CC=CC=C3N=C12)* 0.000 description 1
125000001644 phenoxazinyl group Chemical group C1(=CC=CC=2OC3=CC=CC=C3NC12)* 0.000 description 1
ZUOUZKKEUPVFJK-UHFFFAOYSA-N phenylbenzene Natural products C1=CC=CC=C1C1=CC=CC=C1 ZUOUZKKEUPVFJK-UHFFFAOYSA-N 0.000 description 1
NBIIXXVUZAFLBC-UHFFFAOYSA-K phosphate Chemical compound [O-]P([O-])([O-])=O NBIIXXVUZAFLBC-UHFFFAOYSA-K 0.000 description 1
239000010452 phosphate Substances 0.000 description 1
150000008105 phosphatidylcholines Chemical class 0.000 description 1
UHZYTMXLRWXGPK-UHFFFAOYSA-N phosphorus pentachloride Chemical compound ClP(Cl)(Cl)(Cl)Cl UHZYTMXLRWXGPK-UHFFFAOYSA-N 0.000 description 1
IPNPIHIZVLFAFP-UHFFFAOYSA-N phosphorus tribromide Chemical compound BrP(Br)Br IPNPIHIZVLFAFP-UHFFFAOYSA-N 0.000 description 1
XUWHAWMETYGRKB-UHFFFAOYSA-N piperidin-2-one Chemical compound O=C1CCCCN1 XUWHAWMETYGRKB-UHFFFAOYSA-N 0.000 description 1
CNMOHEDUVVUVPP-UHFFFAOYSA-N piperidine-2,3-dione Chemical compound O=C1CCCNC1=O CNMOHEDUVVUVPP-UHFFFAOYSA-N 0.000 description 1
125000004928 piperidonyl group Chemical group 0.000 description 1
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230000010118 platelet activation Effects 0.000 description 1
229920001610 polycaprolactone Polymers 0.000 description 1
229920000573 polyethylene Polymers 0.000 description 1
239000004626 polylactic acid Substances 0.000 description 1
229920000656 polylysine Polymers 0.000 description 1
229920006324 polyoxymethylene Polymers 0.000 description 1
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229920000036 polyvinylpyrrolidone Polymers 0.000 description 1
239000011591 potassium Substances 0.000 description 1
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239000011698 potassium fluoride Substances 0.000 description 1
235000003270 potassium fluoride Nutrition 0.000 description 1
239000002243 precursor Substances 0.000 description 1
239000003755 preservative agent Substances 0.000 description 1
150000003138 primary alcohols Chemical class 0.000 description 1
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125000004368 propenyl group Chemical group C(=CC)* 0.000 description 1
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230000017854 proteolysis Effects 0.000 description 1
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150000003217 pyrazoles Chemical class 0.000 description 1
125000003072 pyrazolidinyl group Chemical group 0.000 description 1
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LBFMENANQYHPPH-UHFFFAOYSA-N pyrazolo[3,4-c]pyridin-7-one Chemical compound O=C1N=CC=C2C=NN=C12 LBFMENANQYHPPH-UHFFFAOYSA-N 0.000 description 1
DOTPSQVYOBAWPQ-UHFFFAOYSA-N pyrazolo[4,3-d]pyrimidin-3-one Chemical class N1=CN=C2C(=O)N=NC2=C1 DOTPSQVYOBAWPQ-UHFFFAOYSA-N 0.000 description 1
125000002098 pyridazinyl group Chemical group 0.000 description 1
VTGOHKSTWXHQJK-UHFFFAOYSA-N pyrimidin-2-ol Chemical compound OC1=NC=CC=N1 VTGOHKSTWXHQJK-UHFFFAOYSA-N 0.000 description 1
125000001422 pyrrolinyl group Chemical group 0.000 description 1
125000000168 pyrrolyl group Chemical group 0.000 description 1
150000003242 quaternary ammonium salts Chemical class 0.000 description 1
238000010791 quenching Methods 0.000 description 1
230000000171 quenching effect Effects 0.000 description 1
OVSQVDMCBVZWGM-QSOFNFLRSA-N quercetin 3-O-beta-D-glucopyranoside Chemical compound O[C@@H]1[C@@H](O)[C@H](O)[C@@H](CO)O[C@H]1OC1=C(C=2C=C(O)C(O)=CC=2)OC2=CC(O)=CC(O)=C2C1=O OVSQVDMCBVZWGM-QSOFNFLRSA-N 0.000 description 1
125000002294 quinazolinyl group Chemical group N1=C(N=CC2=CC=CC=C12)* 0.000 description 1
IUVKMZGDUIUOCP-BTNSXGMBSA-N quinbolone Chemical compound O([C@H]1CC[C@H]2[C@H]3[C@@H]([C@]4(C=CC(=O)C=C4CC3)C)CC[C@@]21C)C1=CCCC1 IUVKMZGDUIUOCP-BTNSXGMBSA-N 0.000 description 1
125000002943 quinolinyl group Chemical group N1=C(C=CC2=CC=CC=C12)* 0.000 description 1
125000001567 quinoxalinyl group Chemical group N1=C(C=NC2=CC=CC=C12)* 0.000 description 1
125000004621 quinuclidinyl group Chemical group N12C(CC(CC1)CC2)* 0.000 description 1
239000002464 receptor antagonist Substances 0.000 description 1
229940044551 receptor antagonist Drugs 0.000 description 1
238000011084 recovery Methods 0.000 description 1
230000000306 recurrent effect Effects 0.000 description 1
230000011514 reflex Effects 0.000 description 1
238000012552 review Methods 0.000 description 1
229910052702 rhenium Inorganic materials 0.000 description 1
238000007363 ring formation reaction Methods 0.000 description 1
YBCAZPLXEGKKFM-UHFFFAOYSA-K ruthenium(iii) chloride Chemical compound [Cl-].[Cl-].[Cl-].[Ru+3] YBCAZPLXEGKKFM-UHFFFAOYSA-K 0.000 description 1
229960004889 salicylic acid Drugs 0.000 description 1
108010073863 saruplase Proteins 0.000 description 1
125000002914 sec-butyl group Chemical group [H]C([H])([H])C([H])([H])C([H])(*)C([H])([H])[H] 0.000 description 1
JPJALAQPGMAKDF-UHFFFAOYSA-N selenium dioxide Chemical compound O=[Se]=O JPJALAQPGMAKDF-UHFFFAOYSA-N 0.000 description 1
229940076279 serotonin Drugs 0.000 description 1
230000019491 signal transduction Effects 0.000 description 1
150000003384 small molecules Chemical class 0.000 description 1
235000015424 sodium Nutrition 0.000 description 1
229910052708 sodium Inorganic materials 0.000 description 1
235000010413 sodium alginate Nutrition 0.000 description 1
239000000661 sodium alginate Substances 0.000 description 1
229940005550 sodium alginate Drugs 0.000 description 1
WXMKPNITSTVMEF-UHFFFAOYSA-M sodium benzoate Chemical compound [Na+].[O-]C(=O)C1=CC=CC=C1 WXMKPNITSTVMEF-UHFFFAOYSA-M 0.000 description 1
239000004299 sodium benzoate Substances 0.000 description 1
235000010234 sodium benzoate Nutrition 0.000 description 1
235000019812 sodium carboxymethyl cellulose Nutrition 0.000 description 1
229920001027 sodium carboxymethylcellulose Polymers 0.000 description 1
QDRKDTQENPPHOJ-UHFFFAOYSA-N sodium ethoxide Chemical compound [Na+].CC[O-] QDRKDTQENPPHOJ-UHFFFAOYSA-N 0.000 description 1
239000012312 sodium hydride Substances 0.000 description 1
235000010267 sodium hydrogen sulphite Nutrition 0.000 description 1
239000004289 sodium hydrogen sulphite Substances 0.000 description 1
RYYKJJJTJZKILX-UHFFFAOYSA-M sodium octadecanoate Chemical compound [Na+].CCCCCCCCCCCCCCCCCC([O-])=O RYYKJJJTJZKILX-UHFFFAOYSA-M 0.000 description 1
235000010265 sodium sulphite Nutrition 0.000 description 1
239000003549 soybean oil Substances 0.000 description 1
235000012424 soybean oil Nutrition 0.000 description 1
150000003413 spiro compounds Chemical class 0.000 description 1
238000010561 standard procedure Methods 0.000 description 1
239000001119 stannous chloride Substances 0.000 description 1
210000002784 stomach Anatomy 0.000 description 1
229960005202 streptokinase Drugs 0.000 description 1
125000003107 substituted aryl group Chemical group 0.000 description 1
239000005720 sucrose Substances 0.000 description 1
150000008163 sugars Chemical class 0.000 description 1
229950000244 sulfanilic acid Drugs 0.000 description 1
MBGGBVCUIVRRBF-UHFFFAOYSA-N sulfinpyrazone 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 description 1
229960003329 sulfinpyrazone Drugs 0.000 description 1
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239000011593 sulfur Substances 0.000 description 1
MLKXDPUZXIRXEP-MFOYZWKCSA-N sulindac Chemical compound CC1=C(CC(O)=O)C2=CC(F)=CC=C2\C1=C/C1=CC=C(S(C)=O)C=C1 MLKXDPUZXIRXEP-MFOYZWKCSA-N 0.000 description 1
229960000894 sulindac Drugs 0.000 description 1
239000003765 sweetening agent Substances 0.000 description 1
208000024891 symptom Diseases 0.000 description 1
238000010189 synthetic method Methods 0.000 description 1
235000002906 tartaric acid Nutrition 0.000 description 1
239000011975 tartaric acid Substances 0.000 description 1
BNWCETAHAJSBFG-UHFFFAOYSA-N tert-butyl 2-bromoacetate Chemical compound CC(C)(C)OC(=O)CBr BNWCETAHAJSBFG-UHFFFAOYSA-N 0.000 description 1
UGNWTBMOAKPKBL-UHFFFAOYSA-N tetrachloro-1,4-benzoquinone Chemical compound ClC1=C(Cl)C(=O)C(Cl)=C(Cl)C1=O UGNWTBMOAKPKBL-UHFFFAOYSA-N 0.000 description 1
125000003718 tetrahydrofuranyl group Chemical group 0.000 description 1
125000003039 tetrahydroisoquinolinyl group Chemical group C1(NCCC2=CC=CC=C12)* 0.000 description 1
125000001712 tetrahydronaphthyl group Chemical group C1(CCCC2=CC=CC=C12)* 0.000 description 1
125000000147 tetrahydroquinolinyl group Chemical group N1(CCCC2=CC=CC=C12)* 0.000 description 1
UEUXEKPTXMALOB-UHFFFAOYSA-J tetrasodium;2-[2-[bis(carboxylatomethyl)amino]ethyl-(carboxylatomethyl)amino]acetate Chemical compound [Na+].[Na+].[Na+].[Na+].[O-]C(=O)CN(CC([O-])=O)CCN(CC([O-])=O)CC([O-])=O UEUXEKPTXMALOB-UHFFFAOYSA-J 0.000 description 1
150000003536 tetrazoles Chemical class 0.000 description 1
230000001225 therapeutic effect Effects 0.000 description 1
125000004627 thianthrenyl group Chemical group C1(=CC=CC=2SC3=CC=CC=C3SC12)* 0.000 description 1
125000000335 thiazolyl group Chemical group 0.000 description 1
UMGDCJDMYOKAJW-UHFFFAOYSA-N thiourea Chemical class NC(N)=S UMGDCJDMYOKAJW-UHFFFAOYSA-N 0.000 description 1
201000005060 thrombophlebitis Diseases 0.000 description 1
AXZWODMDQAVCJE-UHFFFAOYSA-L tin(II) chloride (anhydrous) Chemical group [Cl-].[Cl-].[Sn+2] AXZWODMDQAVCJE-UHFFFAOYSA-L 0.000 description 1
229960000187 tissue plasminogen activator Drugs 0.000 description 1
230000000699 topical effect Effects 0.000 description 1
235000010487 tragacanth Nutrition 0.000 description 1
239000000196 tragacanth Substances 0.000 description 1
229940116362 tragacanth Drugs 0.000 description 1
201000010875 transient cerebral ischemia Diseases 0.000 description 1
125000005270 trialkylamine group Chemical group 0.000 description 1
125000004306 triazinyl group Chemical group 0.000 description 1
125000003866 trichloromethyl group Chemical group ClC(Cl)(Cl)* 0.000 description 1
UCPYLLCMEDAXFR-UHFFFAOYSA-N triphosgene Chemical compound ClC(Cl)(Cl)OC(=O)OC(Cl)(Cl)Cl UCPYLLCMEDAXFR-UHFFFAOYSA-N 0.000 description 1
LENZDBCJOHFCAS-UHFFFAOYSA-N tris Chemical compound OCC(N)(CO)CO LENZDBCJOHFCAS-UHFFFAOYSA-N 0.000 description 1
229910052722 tritium Inorganic materials 0.000 description 1
108010036927 trypsin-like serine protease Proteins 0.000 description 1
230000006433 tumor necrosis factor production Effects 0.000 description 1
230000007306 turnover Effects 0.000 description 1
MWOOGOJBHIARFG-UHFFFAOYSA-N vanillin Chemical compound COC1=CC(C=O)=CC=C1O MWOOGOJBHIARFG-UHFFFAOYSA-N 0.000 description 1
235000012141 vanillin Nutrition 0.000 description 1
FGQOOHJZONJGDT-UHFFFAOYSA-N vanillin Natural products COC1=CC(O)=CC(C=O)=C1 FGQOOHJZONJGDT-UHFFFAOYSA-N 0.000 description 1
125000000391 vinyl group Chemical group [H]C([*])=C([H])[H] 0.000 description 1
PJVWKTKQMONHTI-UHFFFAOYSA-N warfarin Chemical compound OC=1C2=CC=CC=C2OC(=O)C=1C(CC(=O)C)C1=CC=CC=C1 PJVWKTKQMONHTI-UHFFFAOYSA-N 0.000 description 1
229960005080 warfarin Drugs 0.000 description 1
238000005406 washing Methods 0.000 description 1
239000001993 wax Substances 0.000 description 1
238000005303 weighing Methods 0.000 description 1
239000000230 xanthan gum Substances 0.000 description 1
235000010493 xanthan gum Nutrition 0.000 description 1
229920001285 xanthan gum Polymers 0.000 description 1
229940082509 xanthan gum Drugs 0.000 description 1
125000001834 xanthenyl group Chemical group C1=CC=CC=2OC3=CC=CC=C3C(C12)* 0.000 description 1
BPICBUSOMSTKRF-UHFFFAOYSA-N xylazine Chemical compound CC1=CC=CC(C)=C1NC1=NCCCS1 BPICBUSOMSTKRF-UHFFFAOYSA-N 0.000 description 1
229960001600 xylazine Drugs 0.000 description 1
229930195724 β-lactose Natural products 0.000 description 1

Classifications

- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
- C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
- C07D471/04—Ortho-condensed systems
- 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
- C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
- C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
- C07D487/04—Ortho-condensed systems

Landscapes

Chemical & Material Sciences (AREA)
Organic Chemistry (AREA)
Health & Medical Sciences (AREA)
Engineering & Computer Science (AREA)
Bioinformatics & Cheminformatics (AREA)
Veterinary Medicine (AREA)
Life Sciences & Earth Sciences (AREA)
Public Health (AREA)
Chemical Kinetics & Catalysis (AREA)
General Chemical & Material Sciences (AREA)
Medicinal Chemistry (AREA)
Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
General Health & Medical Sciences (AREA)
Pharmacology & Pharmacy (AREA)
Animal Behavior & Ethology (AREA)
Heart & Thoracic Surgery (AREA)
Cardiology (AREA)
Vascular Medicine (AREA)
Urology & Nephrology (AREA)
Diabetes (AREA)
Hematology (AREA)
Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Nitrogen Condensed Heterocyclic Rings (AREA)
Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)

NO20013072A 1998-12-23 2001-06-20 Nitrogenholdige heterocykler,anvendelse av disse for fremstilling av medikamenter samt farmasoytiske preparater. NO319816B1 (no)

Applications Claiming Priority (3)

Application Number	Priority Date	Filing Date	Title
US11362898P	1998-12-23	1998-12-23
US12763399P	1999-04-02	1999-04-02
PCT/US1999/030316 WO2000039131A1 (fr)	1998-12-23	1999-12-17	Heterobicycliques contenant de l'azote utilises comme inhibiteurs du facteur xa

Publications (3)

Publication Number	Publication Date
NO20013072D0 NO20013072D0 (no)	2001-06-20
NO20013072L NO20013072L (no)	2001-06-20
NO319816B1 true NO319816B1 (no)	2005-09-19

Family

ID=26811284

Family Applications (1)

Application Number	Title	Priority Date	Filing Date
NO20013072A NO319816B1 (no)	1998-12-23	2001-06-20	Nitrogenholdige heterocykler,anvendelse av disse for fremstilling av medikamenter samt farmasoytiske preparater.

Country Status (26)

Country	Link
US (2)	US6413980B1 (fr)
EP (1)	EP1140941B1 (fr)
JP (1)	JP2002533465A (fr)
KR (1)	KR100628407B1 (fr)
CN (1)	CN100340559C (fr)
AR (1)	AR024242A1 (fr)
AT (1)	ATE280171T1 (fr)
AU (1)	AU759711B2 (fr)
BR (1)	BR9917080A (fr)
CA (1)	CA2349330C (fr)
DE (1)	DE69921358T2 (fr)
DK (1)	DK1140941T3 (fr)
EA (1)	EA004515B1 (fr)
ES (1)	ES2232202T3 (fr)
HK (1)	HK1052508B (fr)
HR (1)	HRP990396A2 (fr)
IL (2)	IL142959A0 (fr)
MX (1)	MXPA01006502A (fr)
MY (1)	MY138239A (fr)
NO (1)	NO319816B1 (fr)
NZ (1)	NZ511674A (fr)
PT (1)	PT1140941E (fr)
SI (1)	SI1140941T1 (fr)
TW (1)	TWI225862B (fr)
WO (1)	WO2000039131A1 (fr)
ZA (1)	ZA200103795B (fr)

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US6506771B2 (en)	2000-06-23	2003-01-14	Bristol-Myers Squibb Pharma Company	Heteroaryl-phenyl heterobicyclic factor Xa inhibitors
US20040077605A1 (en) *	2001-06-20	2004-04-22	Salvati Mark E.	Fused heterocyclic succinimide compounds and analogs thereof, modulators of nuclear hormone receptor function
EP1854798A3 (fr)	2000-09-19	2007-11-28	Bristol-Myers Squibb Company	Composés de succinimide hétérocyclique fondu et leurs analogies, modulateurs de la fonction de récepteur d'hormone nucléaire
US20040087548A1 (en)	2001-02-27	2004-05-06	Salvati Mark E.	Fused cyclic succinimide compounds and analogs thereof, modulators of nuclear hormone receptor function
US6960595B2 (en) *	2001-03-23	2005-11-01	Bristol-Myers Squibb Pharma Company	5-6 to 5-7 Heterobicycles as factor Xa inhibitors
WO2002085356A1 (fr) *	2001-04-18	2002-10-31	Bristol-Myers Squibb Company	1, 4, 5, 6-tetrahydropyrazolo-[3, 4-c]-pyridine-7-ones comme inhiteurs du facteur xa
CA2441772A1 (fr)	2001-04-18	2002-10-31	Bristol-Myers Squibb Company	1,4,5,6-tetrahydropyrazolo-¬3,4-c\|-pyridin-7-ones utilisees comme inhibiteurs du facteur xa
EP1414449A4 (fr) *	2001-05-22	2005-04-06	Bristol Myers Squibb Co	Inhibiteurs bicycliques du facteur xa
TWI331526B (en)	2001-09-21	2010-10-11	Bristol Myers Squibb Pharma Co	Lactam-containing compounds and derivatives thereof as factor xa inhibitors
CN101357914A (zh)	2001-09-21	2009-02-04	百时美施贵宝公司	含有内酰胺的化合物及其衍生物作为Xa因子的抑制剂
TW200302225A (en)	2001-12-04	2003-08-01	Bristol Myers Squibb Co	Substituted amino methyl factor Xa inhibitors
AU2002350217A1 (en)	2001-12-04	2003-06-17	Bristol-Myers Squibb Company	Glycinamides as factor xa inhibitors
TW200738672A (en)	2001-12-10	2007-10-16	Bristol Myers Squibb Co	Intermediated for the preparation of 4,5-dihydro-pyrazolo [3,4-c] pyrid-2-ones
EP1467979B1 (fr) *	2001-12-19	2008-08-13	Bristol-Myers Squibb Company	Composes heterocycliques condenses et leurs substances analogues, modulant la fonction du recepteur hormonal nucleaire
US7312214B2 (en)	2002-05-10	2007-12-25	Bristol-Myers Squibb Company	1, 1-disubstituted cycloalkyl derivatives as factor Xa inhibitors
HUE025683T2 (hu)	2002-12-03	2016-04-28	Pharmacyclics Llc	VIIA faktor inhibitor 2-(2-hidroxi-bifenil-3-il)-1H-benzoimidazol-5-karboxamidin-származékok
US7429581B2 (en)	2002-12-23	2008-09-30	Sanofi-Aventis Deutschland Gmbh	Pyrazole-derivatives as factor Xa inhibitors
EP1479678A1 (fr) *	2003-05-19	2004-11-24	Aventis Pharma Deutschland GmbH	Derivés du pyrazole en tant qu'inhibiteurs du facteur Xa
ATE444292T1 (de) *	2002-12-23	2009-10-15	Sanofi Aventis Deutschland	Pyrazolderivate als faktor-xa-inhibitoren
US7135469B2 (en) *	2003-03-18	2006-11-14	Bristol Myers Squibb, Co.	Linear chain substituted monocyclic and bicyclic derivatives as factor Xa inhibitors
US7122557B2 (en) *	2003-03-18	2006-10-17	Bristol-Myers Squibb Company	Sulfonyl-amidino-containing and tetrahydropyrimidino-containing compounds as factor Xa inhibitors
EP1479675A1 (fr) *	2003-05-19	2004-11-24	Aventis Pharma Deutschland GmbH	Derivés d'indazole en tant qu'inhibiteurs du facteur Xa
EP1635823A1 (fr) *	2003-05-20	2006-03-22	TransTech Pharma Inc.	Antagonistes rage utilises contre l'amylose et les maladies associees
US7022850B2 (en)	2003-05-22	2006-04-04	Bristol-Myers Squibb Co.	Bicyclicpyrimidones and their use to treat diseases
JP2007506787A (ja)	2003-09-23	2007-03-22	バーテックス　ファーマシューティカルズ　インコーポレイテッド	プロテインキナーゼインヒビターとしてのピラゾロピロール誘導体
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MXPA01006502A (es)	2002-04-08
EA200100688A1 (ru)	2001-12-24
NO20013072D0 (no)	2001-06-20
AR024242A1 (es)	2002-09-25
BR9917080A (pt)	2002-03-12
EA004515B1 (ru)	2004-04-29
ZA200103795B (en)	2002-08-12
CN1391575A (zh)	2003-01-15
JP2002533465A (ja)	2002-10-08
CA2349330C (fr)	2009-09-29
EP1140941A1 (fr)	2001-10-10
HK1052508A1 (zh)	2003-09-19
MY138239A (en)	2009-05-29
CN100340559C (zh)	2007-10-03
WO2000039131A1 (fr)	2000-07-06
HRP990396A2 (en)	2000-08-31
CA2349330A1 (fr)	2000-07-06
SI1140941T1 (en)	2005-04-30
DE69921358T2 (de)	2006-03-09
EP1140941B1 (fr)	2004-10-20
AU2371700A (en)	2000-07-31
US6413980B1 (en)	2002-07-02
IL142959A0 (en)	2002-04-21
PT1140941E (pt)	2005-02-28
DK1140941T3 (da)	2005-02-14
KR100628407B1 (ko)	2006-09-26
US20030004167A1 (en)	2003-01-02
TWI225862B (en)	2005-01-01
KR20010092754A (ko)	2001-10-26
NO20013072L (no)	2001-06-20
HK1052508B (zh)	2008-08-01
DE69921358D1 (de)	2004-11-25
ES2232202T3 (es)	2005-05-16
ATE280171T1 (de)	2004-11-15
AU759711B2 (en)	2003-04-17
US6673810B2 (en)	2004-01-06
NZ511674A (en)	2003-11-28
IL142959A (en)	2010-05-31

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NO319816B1 (no)	2005-09-19	Nitrogenholdige heterocykler,anvendelse av disse for fremstilling av medikamenter samt farmasoytiske preparater.
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AU747776B2 (en)	2002-05-23	Thrombin inhibitors
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ES2712699T3 (es)	2019-05-14	Tetrahidroisoquinolinas que contienen azoles sustituidos como inhibidores del factor XIa
US20020016326A1 (en)	2002-02-07	Nitrogen containing heteroaromatics with ortho-substituted P1's as factor Xa inhibitors
WO2017072020A1 (fr)	2017-05-04	Utilisation de dérivés hétéroarylcarboxamides comme inhibiteurs de la kallicréine plasmatique
SI20017A (sl)	2000-02-29	Dušik vsebujoči heteroaromati kot inhibitorji faktorja Xa
JP2001526268A (ja)	2001-12-18	Ｘａ因子阻害剤としての、オルト−置換Ｐ１を有する、窒素含有複素環式芳香族化合物
CN112028877A (zh)	2020-12-04	烷氧吡啶酮化合物及其制备方法和用途
CA3229293A1 (fr)	2023-03-16	Derives de 6-aza-quinoleine et utilisations associees
US6858616B2 (en)	2005-02-22	Nitrogen containing heterobicycles as factor Xa inhibitors
NZ626176A (en)	2015-09-25	Pyridinone and pyrimidinone derivatives as factor xia inhibitors
NZ626176B2 (en)	2016-01-06	Pyridinone and pyrimidinone derivatives as factor xia inhibitors

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