IL97521A - The use of Tanidap to inhibit the activation of collagenase and to inhibit the activity of myeloproxidase - Google Patents

The use of Tanidap to inhibit the activation of collagenase and to inhibit the activity of myeloproxidase

Info

Publication number: IL97521A
Authority: IL; Israel
Prior art keywords: tenidap; collagenase; pharmaceutically; hemihydrate; monohydrate
Prior art date: 1990-03-19

Application number

IL9752191A

Other languages

English (en)

Hebrew (he)

Other versions

IL97521A0 (en

Original Assignee

Pfizer

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.)

1990-03-19

Filing date

1991-03-12

Publication date

1995-12-31

1991-03-12 Application filed by Pfizer filed Critical Pfizer

1992-06-21 Publication of IL97521A0 publication Critical patent/IL97521A0/xx

1995-12-31 Publication of IL97521A publication Critical patent/IL97521A/en

Links

229960003676 tenidap Drugs 0.000 title claims description 52
LXIKEPCNDFVJKC-QXMHVHEDSA-N tenidap Chemical compound C12=CC(Cl)=CC=C2N(C(=O)N)C(=O)\C1=C(/O)C1=CC=CS1 LXIKEPCNDFVJKC-QXMHVHEDSA-N 0.000 title claims description 51
102000029816 Collagenase Human genes 0.000 title claims description 47
108060005980 Collagenase Proteins 0.000 title claims description 47
229960002424 collagenase Drugs 0.000 title claims description 47
102000003896 Myeloperoxidases Human genes 0.000 title claims description 21
108090000235 Myeloperoxidases Proteins 0.000 title claims description 21
230000000694 effects Effects 0.000 title claims description 21
230000004913 activation Effects 0.000 title claims description 16
239000003814 drug Substances 0.000 title description 3
150000003839 salts Chemical class 0.000 claims description 41
208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims description 33
241000124008 Mammalia Species 0.000 claims description 25
208000035475 disorder Diseases 0.000 claims description 21
150000004682 monohydrates Chemical class 0.000 claims description 17
230000001404 mediated effect Effects 0.000 claims description 13
201000010099 disease Diseases 0.000 claims description 12
230000002401 inhibitory effect Effects 0.000 claims description 12
239000008194 pharmaceutical composition Substances 0.000 claims description 9
208000006386 Bone Resorption Diseases 0.000 claims description 7
230000024279 bone resorption Effects 0.000 claims description 7
238000002360 preparation method Methods 0.000 claims description 7
206010064996 Ulcerative keratitis Diseases 0.000 claims description 6
208000027866 inflammatory disease Diseases 0.000 claims description 6
238000007911 parenteral administration Methods 0.000 claims description 6
208000028169 periodontal disease Diseases 0.000 claims description 6
208000027418 Wounds and injury Diseases 0.000 claims description 5
239000003112 inhibitor Substances 0.000 claims description 5
206010005949 Bone cancer Diseases 0.000 claims description 3
208000018084 Bone neoplasm Diseases 0.000 claims description 3
208000001132 Osteoporosis Diseases 0.000 claims description 3
239000004480 active ingredient Substances 0.000 claims description 3
230000001394 metastastic effect Effects 0.000 claims description 3
206010061289 metastatic neoplasm Diseases 0.000 claims description 3
238000011200 topical administration Methods 0.000 claims description 2
239000000825 pharmaceutical preparation Substances 0.000 claims 2
239000006228 supernatant Substances 0.000 description 18
239000002585 base Substances 0.000 description 17
150000001875 compounds Chemical class 0.000 description 14
210000000440 neutrophil Anatomy 0.000 description 14
-1 3-substituted-2-oxindole-l-carboxamides Chemical class 0.000 description 10
238000003556 assay Methods 0.000 description 9
238000011534 incubation Methods 0.000 description 9
210000004027 cell Anatomy 0.000 description 8
LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 description 6
DNIAPMSPPWPWGF-UHFFFAOYSA-N Propylene glycol Chemical compound CC(O)CO DNIAPMSPPWPWGF-UHFFFAOYSA-N 0.000 description 6
HEMHJVSKTPXQMS-UHFFFAOYSA-M Sodium hydroxide Chemical compound [OH-].[Na+] HEMHJVSKTPXQMS-UHFFFAOYSA-M 0.000 description 6
230000005764 inhibitory process Effects 0.000 description 6
238000000034 method Methods 0.000 description 6
XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 description 6
102000008186 Collagen Human genes 0.000 description 5
108010035532 Collagen Proteins 0.000 description 5
229920001436 collagen Polymers 0.000 description 5
HZAXFHJVJLSVMW-UHFFFAOYSA-N 2-Aminoethan-1-ol Chemical compound NCCO HZAXFHJVJLSVMW-UHFFFAOYSA-N 0.000 description 4
QGZKDVFQNNGYKY-UHFFFAOYSA-N Ammonia Chemical compound N QGZKDVFQNNGYKY-UHFFFAOYSA-N 0.000 description 4
108091003079 Bovine Serum Albumin Proteins 0.000 description 4
239000012981 Hank's balanced salt solution Substances 0.000 description 4
MHAJPDPJQMAIIY-UHFFFAOYSA-N Hydrogen peroxide Chemical compound OO MHAJPDPJQMAIIY-UHFFFAOYSA-N 0.000 description 4
206010052428 Wound Diseases 0.000 description 4
229940098773 bovine serum albumin Drugs 0.000 description 4
239000003085 diluting agent Substances 0.000 description 4
CGIGDMFJXJATDK-UHFFFAOYSA-N indomethacin Chemical compound CC1=C(CC(O)=O)C2=CC(OC)=CC=C2N1C(=O)C1=CC=C(Cl)C=C1 CGIGDMFJXJATDK-UHFFFAOYSA-N 0.000 description 4
239000000203 mixture Substances 0.000 description 4
239000000243 solution Substances 0.000 description 4
WVDDGKGOMKODPV-UHFFFAOYSA-N Benzyl alcohol Chemical compound OCC1=CC=CC=C1 WVDDGKGOMKODPV-UHFFFAOYSA-N 0.000 description 3
HEFNNWSXXWATRW-UHFFFAOYSA-N Ibuprofen Chemical compound CC(C)CC1=CC=C(C(C)C(O)=O)C=C1 HEFNNWSXXWATRW-UHFFFAOYSA-N 0.000 description 3
GUBGYTABKSRVRQ-QKKXKWKRSA-N Lactose Natural products OC[C@H]1O[C@@H](O[C@H]2[C@H](O)[C@@H](O)C(O)O[C@@H]2CO)[C@H](O)[C@@H](O)[C@H]1O GUBGYTABKSRVRQ-QKKXKWKRSA-N 0.000 description 3
SJRJJKPEHAURKC-UHFFFAOYSA-N N-Methylmorpholine Chemical compound CN1CCOCC1 SJRJJKPEHAURKC-UHFFFAOYSA-N 0.000 description 3
AFBPFSWMIHJQDM-UHFFFAOYSA-N N-methyl-N-phenylamine Natural products CNC1=CC=CC=C1 AFBPFSWMIHJQDM-UHFFFAOYSA-N 0.000 description 3
CMWTZPSULFXXJA-UHFFFAOYSA-N Naproxen Natural products C1=C(C(C)C(O)=O)C=CC2=CC(OC)=CC=C21 CMWTZPSULFXXJA-UHFFFAOYSA-N 0.000 description 3
RWRDLPDLKQPQOW-UHFFFAOYSA-N Pyrrolidine Chemical compound C1CCNC1 RWRDLPDLKQPQOW-UHFFFAOYSA-N 0.000 description 3
FAPWRFPIFSIZLT-UHFFFAOYSA-M Sodium chloride Chemical compound [Na+].[Cl-] FAPWRFPIFSIZLT-UHFFFAOYSA-M 0.000 description 3
ZMANZCXQSJIPKH-UHFFFAOYSA-N Triethylamine Chemical compound CCN(CC)CC ZMANZCXQSJIPKH-UHFFFAOYSA-N 0.000 description 3
229910052784 alkaline earth metal Inorganic materials 0.000 description 3
239000007864 aqueous solution Substances 0.000 description 3
230000001580 bacterial effect Effects 0.000 description 3
239000006285 cell suspension Substances 0.000 description 3
238000005119 centrifugation Methods 0.000 description 3
MUCZHBLJLSDCSD-UHFFFAOYSA-N diisopropyl fluorophosphate Chemical compound CC(C)OP(F)(=O)OC(C)C MUCZHBLJLSDCSD-UHFFFAOYSA-N 0.000 description 3
239000002552 dosage form Substances 0.000 description 3
229960005051 fluostigmine Drugs 0.000 description 3
239000000499 gel Substances 0.000 description 3
229960001680 ibuprofen Drugs 0.000 description 3
239000007788 liquid Substances 0.000 description 3
229960002009 naproxen Drugs 0.000 description 3
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 description 3
229960002702 piroxicam Drugs 0.000 description 3
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 description 3
159000000000 sodium salts Chemical class 0.000 description 3
238000011282 treatment Methods 0.000 description 3
PAYRUJLWNCNPSJ-UHFFFAOYSA-N Aniline Chemical compound NC1=CC=CC=C1 PAYRUJLWNCNPSJ-UHFFFAOYSA-N 0.000 description 2
VTYYLEPIZMXCLO-UHFFFAOYSA-L Calcium carbonate Chemical compound [Ca+2].[O-]C([O-])=O VTYYLEPIZMXCLO-UHFFFAOYSA-L 0.000 description 2
102000004190 Enzymes Human genes 0.000 description 2
108090000790 Enzymes Proteins 0.000 description 2
PEDCQBHIVMGVHV-UHFFFAOYSA-N Glycerine Chemical compound OCC(O)CO PEDCQBHIVMGVHV-UHFFFAOYSA-N 0.000 description 2
102000003820 Lipoxygenases Human genes 0.000 description 2
108090000128 Lipoxygenases Proteins 0.000 description 2
YNAVUWVOSKDBBP-UHFFFAOYSA-N Morpholine Chemical compound C1COCCN1 YNAVUWVOSKDBBP-UHFFFAOYSA-N 0.000 description 2
102000035195 Peptidases Human genes 0.000 description 2
108091005804 Peptidases Proteins 0.000 description 2
NQRYJNQNLNOLGT-UHFFFAOYSA-N Piperidine Chemical compound C1CCNCC1 NQRYJNQNLNOLGT-UHFFFAOYSA-N 0.000 description 2
102000004005 Prostaglandin-endoperoxide synthases Human genes 0.000 description 2
108090000459 Prostaglandin-endoperoxide synthases Proteins 0.000 description 2
239000004365 Protease Substances 0.000 description 2
241000219061 Rheum Species 0.000 description 2
CDBYLPFSWZWCQE-UHFFFAOYSA-L Sodium Carbonate Chemical compound [Na+].[Na+].[O-]C([O-])=O CDBYLPFSWZWCQE-UHFFFAOYSA-L 0.000 description 2
PXIPVTKHYLBLMZ-UHFFFAOYSA-N Sodium azide Chemical compound [Na+].[N-]=[N+]=[N-] PXIPVTKHYLBLMZ-UHFFFAOYSA-N 0.000 description 2
229920002472 Starch Polymers 0.000 description 2
210000001744 T-lymphocyte Anatomy 0.000 description 2
GSEJCLTVZPLZKY-UHFFFAOYSA-N Triethanolamine Chemical compound OCCN(CCO)CCO GSEJCLTVZPLZKY-UHFFFAOYSA-N 0.000 description 2
229910052783 alkali metal Inorganic materials 0.000 description 2
229910021529 ammonia Inorganic materials 0.000 description 2
206010003246 arthritis Diseases 0.000 description 2
WGQKYBSKWIADBV-UHFFFAOYSA-N benzylamine Chemical compound NCC1=CC=CC=C1 WGQKYBSKWIADBV-UHFFFAOYSA-N 0.000 description 2
230000015572 biosynthetic process Effects 0.000 description 2
230000003833 cell viability Effects 0.000 description 2
239000006071 cream Substances 0.000 description 2
PAFZNILMFXTMIY-UHFFFAOYSA-N cyclohexylamine Chemical compound NC1CCCCC1 PAFZNILMFXTMIY-UHFFFAOYSA-N 0.000 description 2
230000009089 cytolysis Effects 0.000 description 2
ZBCBWPMODOFKDW-UHFFFAOYSA-N diethanolamine Chemical compound OCCNCCO ZBCBWPMODOFKDW-UHFFFAOYSA-N 0.000 description 2
239000003995 emulsifying agent Substances 0.000 description 2
229940088598 enzyme Drugs 0.000 description 2
238000002474 experimental method Methods 0.000 description 2
WQYVRQLZKVEZGA-UHFFFAOYSA-N hypochlorite Chemical compound Cl[O-] WQYVRQLZKVEZGA-UHFFFAOYSA-N 0.000 description 2
QWPPOHNGKGFGJK-UHFFFAOYSA-N hypochlorous acid Chemical compound ClO QWPPOHNGKGFGJK-UHFFFAOYSA-N 0.000 description 2
229960000905 indomethacin Drugs 0.000 description 2
239000006210 lotion Substances 0.000 description 2
HQKMJHAJHXVSDF-UHFFFAOYSA-L magnesium stearate Chemical compound [Mg+2].CCCCCCCCCCCCCCCCCC([O-])=O.CCCCCCCCCCCCCCCCCC([O-])=O HQKMJHAJHXVSDF-UHFFFAOYSA-L 0.000 description 2
239000000463 material Substances 0.000 description 2
229960000224 mersalyl Drugs 0.000 description 2
239000002674 ointment Substances 0.000 description 2
RZXMPPFPUUCRFN-UHFFFAOYSA-N p-toluidine Chemical compound CC1=CC=C(N)C=C1 RZXMPPFPUUCRFN-UHFFFAOYSA-N 0.000 description 2
BWHMMNNQKKPAPP-UHFFFAOYSA-L potassium carbonate Chemical compound [K+].[K+].[O-]C([O-])=O BWHMMNNQKKPAPP-UHFFFAOYSA-L 0.000 description 2
239000000047 product Substances 0.000 description 2
WGYKZJWCGVVSQN-UHFFFAOYSA-N propylamine Chemical compound CCCN WGYKZJWCGVVSQN-UHFFFAOYSA-N 0.000 description 2
238000000746 purification Methods 0.000 description 2
239000011780 sodium chloride Substances 0.000 description 2
QGGPRJRKWYRGKR-UHFFFAOYSA-M sodium;[3-[[2-(carboxylatomethoxy)benzoyl]amino]-2-methoxypropyl]mercury;hydrate Chemical group O.[Na+].COC(C[Hg])CNC(=O)C1=CC=CC=C1OCC([O-])=O QGGPRJRKWYRGKR-UHFFFAOYSA-M 0.000 description 2
239000008107 starch Substances 0.000 description 2
235000019698 starch Nutrition 0.000 description 2
210000001519 tissue Anatomy 0.000 description 2
LJRDOKAZOAKLDU-UDXJMMFXSA-N (2s,3s,4r,5r,6r)-5-amino-2-(aminomethyl)-6-[(2r,3s,4r,5s)-5-[(1r,2r,3s,5r,6s)-3,5-diamino-2-[(2s,3r,4r,5s,6r)-3-amino-4,5-dihydroxy-6-(hydroxymethyl)oxan-2-yl]oxy-6-hydroxycyclohexyl]oxy-4-hydroxy-2-(hydroxymethyl)oxolan-3-yl]oxyoxane-3,4-diol;sulfuric ac Chemical compound OS(O)(=O)=O.N[C@@H]1[C@@H](O)[C@H](O)[C@H](CN)O[C@@H]1O[C@H]1[C@@H](O)[C@H](O[C@H]2[C@@H]([C@@H](N)C[C@@H](N)[C@@H]2O)O[C@@H]2[C@@H]([C@@H](O)[C@H](O)[C@@H](CO)O2)N)O[C@@H]1CO LJRDOKAZOAKLDU-UDXJMMFXSA-N 0.000 description 1
CPOBTYJRKAJERX-UHFFFAOYSA-N 3-ethyl-n-[(3-ethyl-1,3-benzothiazol-2-ylidene)amino]-1,3-benzothiazol-2-imine Chemical compound S1C2=CC=CC=C2N(CC)C1=NN=C1SC2=CC=CC=C2N1CC CPOBTYJRKAJERX-UHFFFAOYSA-N 0.000 description 1
CSDQQAQKBAQLLE-UHFFFAOYSA-N 4-(4-chlorophenyl)-4,5,6,7-tetrahydrothieno[3,2-c]pyridine Chemical compound C1=CC(Cl)=CC=C1C1C(C=CS2)=C2CCN1 CSDQQAQKBAQLLE-UHFFFAOYSA-N 0.000 description 1
IGPDWKCUDHIIRL-UHFFFAOYSA-N 5-chloro-2-oxo-3-[oxo(thiophen-2-yl)methyl]-3H-indole-1-carboxamide Chemical compound C12=CC(Cl)=CC=C2N(C(=O)N)C(=O)C1C(=O)C1=CC=CS1 IGPDWKCUDHIIRL-UHFFFAOYSA-N 0.000 description 1
GUBGYTABKSRVRQ-XLOQQCSPSA-N Alpha-Lactose Chemical compound O[C@@H]1[C@@H](O)[C@@H](O)[C@@H](CO)O[C@H]1O[C@@H]1[C@@H](CO)O[C@H](O)[C@H](O)[C@H]1O GUBGYTABKSRVRQ-XLOQQCSPSA-N 0.000 description 1
QGZKDVFQNNGYKY-UHFFFAOYSA-O Ammonium Chemical compound [NH4+] QGZKDVFQNNGYKY-UHFFFAOYSA-O 0.000 description 1
208000023275 Autoimmune disease Diseases 0.000 description 1
LSNNMFCWUKXFEE-UHFFFAOYSA-M Bisulfite Chemical compound OS([O-])=O LSNNMFCWUKXFEE-UHFFFAOYSA-M 0.000 description 1
241000819038 Chichester Species 0.000 description 1
241001112695 Clostridiales Species 0.000 description 1
102000012422 Collagen Type I Human genes 0.000 description 1
108010022452 Collagen Type I Proteins 0.000 description 1
229920002307 Dextran Polymers 0.000 description 1
235000019739 Dicalciumphosphate Nutrition 0.000 description 1
229920001917 Ficoll Polymers 0.000 description 1
108010010803 Gelatin Proteins 0.000 description 1
WQZGKKKJIJFFOK-GASJEMHNSA-N Glucose Natural products OC[C@H]1OC(O)[C@H](O)[C@@H](O)[C@@H]1O WQZGKKKJIJFFOK-GASJEMHNSA-N 0.000 description 1
239000004705 High-molecular-weight polyethylene Substances 0.000 description 1
DGAQECJNVWCQMB-PUAWFVPOSA-M Ilexoside XXIX Chemical compound C[C@@H]1CC[C@@]2(CC[C@@]3(C(=CC[C@H]4[C@]3(CC[C@@H]5[C@@]4(CC[C@@H](C5(C)C)OS(=O)(=O)[O-])C)C)[C@@H]2[C@]1(C)O)C)C(=O)O[C@H]6[C@@H]([C@H]([C@@H]([C@H](O6)CO)O)O)O.[Na+] DGAQECJNVWCQMB-PUAWFVPOSA-M 0.000 description 1
102000000589 Interleukin-1 Human genes 0.000 description 1
108010002352 Interleukin-1 Proteins 0.000 description 1
208000012659 Joint disease Diseases 0.000 description 1
239000005909 Kieselgur Substances 0.000 description 1
240000007472 Leucaena leucocephala Species 0.000 description 1
235000010643 Leucaena leucocephala Nutrition 0.000 description 1
240000003183 Manihot esculenta Species 0.000 description 1
235000016735 Manihot esculenta subsp esculenta Nutrition 0.000 description 1
HTLZVHNRZJPSMI-UHFFFAOYSA-N N-ethylpiperidine Chemical compound CCN1CCCCC1 HTLZVHNRZJPSMI-UHFFFAOYSA-N 0.000 description 1
MBBZMMPHUWSWHV-BDVNFPICSA-N N-methylglucamine Chemical compound CNC[C@H](O)[C@@H](O)[C@H](O)[C@H](O)CO MBBZMMPHUWSWHV-BDVNFPICSA-N 0.000 description 1
102000056189 Neutrophil collagenases Human genes 0.000 description 1
108030001564 Neutrophil collagenases Proteins 0.000 description 1
235000019483 Peanut oil Nutrition 0.000 description 1
ZLMJMSJWJFRBEC-UHFFFAOYSA-N Potassium Chemical compound [K] ZLMJMSJWJFRBEC-UHFFFAOYSA-N 0.000 description 1
102000012479 Serine Proteases Human genes 0.000 description 1
108010022999 Serine Proteases Proteins 0.000 description 1
244000000231 Sesamum indicum Species 0.000 description 1
VYPSYNLAJGMNEJ-UHFFFAOYSA-N Silicium dioxide Chemical compound O=[Si]=O VYPSYNLAJGMNEJ-UHFFFAOYSA-N 0.000 description 1
KEAYESYHFKHZAL-UHFFFAOYSA-N Sodium Chemical compound [Na] KEAYESYHFKHZAL-UHFFFAOYSA-N 0.000 description 1
DBMJMQXJHONAFJ-UHFFFAOYSA-M Sodium laurylsulphate Chemical compound [Na+].CCCCCCCCCCCCOS([O-])(=O)=O DBMJMQXJHONAFJ-UHFFFAOYSA-M 0.000 description 1
244000061456 Solanum tuberosum Species 0.000 description 1
235000002595 Solanum tuberosum Nutrition 0.000 description 1
229930006000 Sucrose Natural products 0.000 description 1
CZMRCDWAGMRECN-UGDNZRGBSA-N Sucrose Chemical compound O[C@H]1[C@H](O)[C@@H](CO)O[C@@]1(CO)O[C@@H]1[C@H](O)[C@@H](O)[C@H](O)[C@@H](CO)O1 CZMRCDWAGMRECN-UGDNZRGBSA-N 0.000 description 1
238000002835 absorbance Methods 0.000 description 1
230000002378 acidificating effect Effects 0.000 description 1
230000003213 activating effect Effects 0.000 description 1
239000000783 alginic acid Substances 0.000 description 1
235000010443 alginic acid Nutrition 0.000 description 1
229920000615 alginic acid Polymers 0.000 description 1
229960001126 alginic acid Drugs 0.000 description 1
150000004781 alginic acids Chemical class 0.000 description 1
229910000288 alkali metal carbonate Inorganic materials 0.000 description 1
150000008041 alkali metal carbonates Chemical class 0.000 description 1
229910000102 alkali metal hydride Inorganic materials 0.000 description 1
150000008046 alkali metal hydrides Chemical class 0.000 description 1
150000008044 alkali metal hydroxides Chemical class 0.000 description 1
229910001860 alkaline earth metal hydroxide Inorganic materials 0.000 description 1
150000001342 alkaline earth metals Chemical class 0.000 description 1
150000004703 alkoxides Chemical class 0.000 description 1
150000001412 amines Chemical class 0.000 description 1
239000000730 antalgic agent Substances 0.000 description 1
239000012736 aqueous medium Substances 0.000 description 1
239000007900 aqueous suspension Substances 0.000 description 1
239000010425 asbestos Substances 0.000 description 1
235000019445 benzyl alcohol Nutrition 0.000 description 1
WQZGKKKJIJFFOK-VFUOTHLCSA-N beta-D-glucose Chemical compound OC[C@H]1O[C@@H](O)[C@H](O)[C@@H](O)[C@@H]1O WQZGKKKJIJFFOK-VFUOTHLCSA-N 0.000 description 1
239000011230 binding agent Substances 0.000 description 1
210000004369 blood Anatomy 0.000 description 1
239000008280 blood Substances 0.000 description 1
239000000872 buffer Substances 0.000 description 1
HQABUPZFAYXKJW-UHFFFAOYSA-N butan-1-amine Chemical compound CCCCN HQABUPZFAYXKJW-UHFFFAOYSA-N 0.000 description 1
229910000019 calcium carbonate Inorganic materials 0.000 description 1
239000001506 calcium phosphate Substances 0.000 description 1
150000004649 carbonic acid derivatives Chemical class 0.000 description 1
239000000969 carrier Substances 0.000 description 1
230000008859 change Effects 0.000 description 1
238000004040 coloring Methods 0.000 description 1
210000002808 connective tissue Anatomy 0.000 description 1
230000002939 deleterious effect Effects 0.000 description 1
NEFBYIFKOOEVPA-UHFFFAOYSA-K dicalcium phosphate Chemical compound [Ca+2].[Ca+2].[O-]P([O-])([O-])=O NEFBYIFKOOEVPA-UHFFFAOYSA-K 0.000 description 1
229940038472 dicalcium phosphate Drugs 0.000 description 1
229910000390 dicalcium phosphate Inorganic materials 0.000 description 1
HPNMFZURTQLUMO-UHFFFAOYSA-N diethylamine Chemical compound CCNCC HPNMFZURTQLUMO-UHFFFAOYSA-N 0.000 description 1
239000007884 disintegrant Substances 0.000 description 1
239000012153 distilled water Substances 0.000 description 1
229940079593 drug Drugs 0.000 description 1
239000003937 drug carrier Substances 0.000 description 1
239000000975 dye Substances 0.000 description 1
230000004064 dysfunction Effects 0.000 description 1
230000001804 emulsifying effect Effects 0.000 description 1
230000002708 enhancing effect Effects 0.000 description 1
239000000945 filler Substances 0.000 description 1
239000000796 flavoring agent Substances 0.000 description 1
239000012530 fluid Substances 0.000 description 1
230000004907 flux Effects 0.000 description 1
235000013355 food flavoring agent Nutrition 0.000 description 1
235000003599 food sweetener Nutrition 0.000 description 1
238000009472 formulation Methods 0.000 description 1
239000008273 gelatin Substances 0.000 description 1
229920000159 gelatin Polymers 0.000 description 1
239000007903 gelatin capsule Substances 0.000 description 1
235000019322 gelatine Nutrition 0.000 description 1
235000011852 gelatine desserts Nutrition 0.000 description 1
239000011521 glass Substances 0.000 description 1
239000008103 glucose Substances 0.000 description 1
235000011187 glycerol Nutrition 0.000 description 1
150000002344 gold compounds Chemical class 0.000 description 1
239000008187 granular material Substances 0.000 description 1
150000004678 hydrides Chemical class 0.000 description 1
150000004679 hydroxides Chemical class 0.000 description 1
230000002757 inflammatory effect Effects 0.000 description 1
238000007918 intramuscular administration Methods 0.000 description 1
238000010255 intramuscular injection Methods 0.000 description 1
239000007927 intramuscular injection Substances 0.000 description 1
238000007912 intraperitoneal administration Methods 0.000 description 1
238000001990 intravenous administration Methods 0.000 description 1
238000010253 intravenous injection Methods 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
MIKKOBKEXMRYFQ-WZTVWXICSA-N meglumine amidotrizoate Chemical compound C[NH2+]C[C@H](O)[C@@H](O)[C@H](O)[C@H](O)CO.CC(=O)NC1=C(I)C(NC(C)=O)=C(I)C(C([O-])=O)=C1I MIKKOBKEXMRYFQ-WZTVWXICSA-N 0.000 description 1
239000002207 metabolite Substances 0.000 description 1
239000002480 mineral oil Substances 0.000 description 1
235000010446 mineral oil Nutrition 0.000 description 1
210000000056 organ Anatomy 0.000 description 1
230000001590 oxidative effect Effects 0.000 description 1
230000001575 pathological effect Effects 0.000 description 1
239000000312 peanut oil Substances 0.000 description 1
239000003961 penetration enhancing agent Substances 0.000 description 1
229960001639 penicillamine Drugs 0.000 description 1
239000000546 pharmaceutical excipient Substances 0.000 description 1
229920001223 polyethylene glycol Polymers 0.000 description 1
239000001267 polyvinylpyrrolidone Substances 0.000 description 1
229920000036 polyvinylpyrrolidone Polymers 0.000 description 1
235000013855 polyvinylpyrrolidone Nutrition 0.000 description 1
229910052573 porcelain Inorganic materials 0.000 description 1
229910052700 potassium Inorganic materials 0.000 description 1
239000011591 potassium Substances 0.000 description 1
229910000027 potassium carbonate Inorganic materials 0.000 description 1
BDAWXSQJJCIFIK-UHFFFAOYSA-N potassium methoxide Chemical compound [K+].[O-]C BDAWXSQJJCIFIK-UHFFFAOYSA-N 0.000 description 1
150000003141 primary amines Chemical class 0.000 description 1
239000002599 prostaglandin synthase inhibitor Substances 0.000 description 1
230000004044 response Effects 0.000 description 1
229910052895 riebeckite Inorganic materials 0.000 description 1
150000003335 secondary amines Chemical class 0.000 description 1
238000004062 sedimentation Methods 0.000 description 1
230000035945 sensitivity Effects 0.000 description 1
239000008159 sesame oil Substances 0.000 description 1
235000011803 sesame oil Nutrition 0.000 description 1
150000004760 silicates Chemical class 0.000 description 1
239000011734 sodium Substances 0.000 description 1
229910052708 sodium Inorganic materials 0.000 description 1
239000007974 sodium acetate buffer Substances 0.000 description 1
229910000029 sodium carbonate Inorganic materials 0.000 description 1
239000001509 sodium citrate Substances 0.000 description 1
NLJMYIDDQXHKNR-UHFFFAOYSA-K sodium citrate Chemical compound O.O.[Na+].[Na+].[Na+].[O-]C(=O)CC(O)(CC([O-])=O)C([O-])=O NLJMYIDDQXHKNR-UHFFFAOYSA-K 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
229910000104 sodium hydride Inorganic materials 0.000 description 1
235000019333 sodium laurylsulphate Nutrition 0.000 description 1
239000008247 solid mixture Substances 0.000 description 1
239000012453 solvate Substances 0.000 description 1
241000894007 species Species 0.000 description 1
238000010561 standard procedure Methods 0.000 description 1
238000007920 subcutaneous administration Methods 0.000 description 1
238000010254 subcutaneous injection Methods 0.000 description 1
239000007929 subcutaneous injection Substances 0.000 description 1
239000000126 substance Substances 0.000 description 1
239000000758 substrate Substances 0.000 description 1
239000005720 sucrose Substances 0.000 description 1
239000000829 suppository Substances 0.000 description 1
239000000375 suspending agent Substances 0.000 description 1
238000013268 sustained release Methods 0.000 description 1
239000012730 sustained-release form Substances 0.000 description 1
239000003765 sweetening agent Substances 0.000 description 1
230000009885 systemic effect Effects 0.000 description 1
239000000454 talc Substances 0.000 description 1
229910052623 talc Inorganic materials 0.000 description 1
235000012222 talc Nutrition 0.000 description 1
150000003512 tertiary amines Chemical class 0.000 description 1
230000000699 topical effect Effects 0.000 description 1

Classifications

- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
- A61K31/403—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with carbocyclic rings, e.g. carbazole
- A61K31/404—Indoles, e.g. pindolol
- A61K31/405—Indole-alkanecarboxylic acids; Derivatives thereof, e.g. tryptophan, indomethacin
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/02—Stomatological preparations, e.g. drugs for caries, aphtae, periodontitis
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P19/00—Drugs for skeletal disorders
- A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
- A61P19/10—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease for osteoporosis
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P27/00—Drugs for disorders of the senses
- A61P27/02—Ophthalmic agents
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00

Landscapes

Health & Medical Sciences (AREA)
General Health & Medical Sciences (AREA)
Pharmacology & Pharmacy (AREA)
Chemical & Material Sciences (AREA)
Public Health (AREA)
Veterinary Medicine (AREA)
Medicinal Chemistry (AREA)
Animal Behavior & Ethology (AREA)
Life Sciences & Earth Sciences (AREA)
Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
Organic Chemistry (AREA)
General Chemical & Material Sciences (AREA)
Chemical Kinetics & Catalysis (AREA)
Bioinformatics & Cheminformatics (AREA)
Engineering & Computer Science (AREA)
Epidemiology (AREA)
Physical Education & Sports Medicine (AREA)
Rheumatology (AREA)
Orthopedic Medicine & Surgery (AREA)
Hematology (AREA)
Obesity (AREA)
Diabetes (AREA)
Ophthalmology & Optometry (AREA)
Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Plural Heterocyclic Compounds (AREA)

IL9752191A 1990-03-19 1991-03-12 The use of Tanidap to inhibit the activation of collagenase and to inhibit the activity of myeloproxidase IL97521A (en)

Applications Claiming Priority (1)

Application Number	Priority Date	Filing Date	Title
US07/495,868 US5008283A (en)	1990-03-19	1990-03-19	Use of tenidap to inhibit activation of collagenase and to inhibit the activity of myeloperoxidase

Publications (2)

Publication Number	Publication Date
IL97521A0 IL97521A0 (en)	1992-06-21
IL97521A true IL97521A (en)	1995-12-31

Family

ID=23970312

Family Applications (1)

Application Number	Title	Priority Date	Filing Date
IL9752191A IL97521A (en)	1990-03-19	1991-03-12	The use of Tanidap to inhibit the activation of collagenase and to inhibit the activity of myeloproxidase

Country Status (14)

Country	Link
US (1)	US5008283A (pt)
EP (1)	EP0448253A3 (pt)
JP (1)	JPH04234815A (pt)
KR (1)	KR930010581B1 (pt)
AU (2)	AU625409B2 (pt)
CA (1)	CA2038409C (pt)
HU (1)	HUT60623A (pt)
IE (1)	IE910860A1 (pt)
IL (1)	IL97521A (pt)
MY (1)	MY107235A (pt)
NZ (1)	NZ237451A (pt)
PT (1)	PT97061B (pt)
SG (1)	SG48397A1 (pt)
ZA (1)	ZA911979B (pt)

Families Citing this family (11)

* Cited by examiner, † Cited by third party
Publication number	Priority date	Publication date	Assignee	Title
US5122534A (en) *	1991-02-08	1992-06-16	Pfizer Inc.	Use of tenidap to reduce total serum cholesterol, ldl cholesterol and triglycerides
TW438798B (en) *	1992-10-07	2001-06-07	Pfizer	3-substituted 2-oxindole-1-carboxamide pharmaceutical compositions
US5298522A (en) *	1993-01-22	1994-03-29	Pfizer Inc.	6-chloro-5-fluoro-3-(2-thenoyl)-2-oxindole-1-carboxamide as an analgesic and anti-inflammatory agent while maintaining a normal urine protein/creatinine ratio
ES2076106B1 (es) *	1993-08-26	1996-06-16	Pfizer	Composiciones farmaceuticas a base de 2-oxindol-1-carboxamidas 3-sustituidas
US5795902A (en) *	1993-09-02	1998-08-18	Pfizer Inc.	3-substituted 2-oxindole-1 carboxamide pharmaceutical compositions
US5516699A (en) *	1994-02-16	1996-05-14	Institute Of Molecular Biology, Inc.	Pyridinoline crosslinks as markers of periodontal and peri-implant disease activity
US5545656A (en) *	1995-04-05	1996-08-13	Pfizer Inc.	2-Oxidole-1-carboxamide pharmaceutical agents for the treatment of alzheimer's disease
US5827840A (en) *	1996-08-01	1998-10-27	The Research Foundation Of State University Of New York	Promotion of wound healing by chemically-modified tetracyclines
AU4084599A (en) *	1998-05-18	1999-12-06	Oklahoma Medical Research Foundation	Resveratrol inhibition of myeloperoxidase
US6544556B1 (en)	2000-09-11	2003-04-08	Andrx Corporation	Pharmaceutical formulations containing a non-steroidal antiinflammatory drug and a proton pump inhibitor
PT2026651E (pt)	2006-03-08	2013-06-04	Cortria Corp	Terapia combinada com inibidores cox não selectivos para prevenir lesões gástricas relacionadas com a cox

Family Cites Families (8)

* Cited by examiner, † Cited by third party
Publication number	Priority date	Publication date	Assignee	Title
US4556672A (en) *	1984-03-19	1985-12-03	Pfizer Inc.	3-Substituted 2-oxindole-1-carboxamides as analgesic and anti-inflammatory agents
US4678802A (en) *	1985-07-09	1987-07-07	Pfizer Inc.	1-acylcarbamoyloxindole-3-carboxamides as antiinflammatory agents
RO105052B1 (en) *	1987-02-02	1994-12-01	Pfizer	Producing process for the crystalline sodium salt, anhydre, of 5-chlorine-3-(2-tenoil)-2-oxindol-1-carboxamide
DE3852145T2 (de) *	1987-02-18	1995-04-06	Beecham Group Plc	Indolderivate, Verfahren zu deren Herstellung und pharmazeutische Präparate, die diese enthalten.
US4853409A (en) *	1988-04-13	1989-08-01	Pfizer Inc.	3-substituted-2-oxindole-1-carboxamides for suppressing T-cell function
US4861794A (en) *	1988-04-13	1989-08-29	Pfizer Inc.	3-substituted-2-oxindole-1-carboxamides as inhibitors of interleukin-1 biosynthesis
DE3814504A1 (de) *	1988-04-29	1989-11-09	Bayer Ag	(alpha)-substituierte 4-(chinolin-2-yl-methoxy)phenylessigsaeuren und -ester, verfahren zu ihrer herstellung und ihre verwendung in arzneimitteln
US5006547A (en) *	1990-03-19	1991-04-09	Pfizer Inc.	Tenidap as an inhibitor of the release of elastase by neutrophils

1990
- 1990-03-19 US US07/495,868 patent/US5008283A/en not_active Expired - Lifetime
1991
- 1991-03-07 EP EP19910301890 patent/EP0448253A3/en not_active Withdrawn
- 1991-03-07 SG SG1996009351A patent/SG48397A1/en unknown
- 1991-03-12 IL IL9752191A patent/IL97521A/en not_active IP Right Cessation
- 1991-03-15 IE IE086091A patent/IE910860A1/en unknown
- 1991-03-15 NZ NZ237451A patent/NZ237451A/en unknown
- 1991-03-15 CA CA002038409A patent/CA2038409C/en not_active Expired - Fee Related
- 1991-03-18 PT PT97061A patent/PT97061B/pt not_active IP Right Cessation
- 1991-03-18 HU HU91872A patent/HUT60623A/hu unknown
- 1991-03-18 AU AU73587/91A patent/AU625409B2/en not_active Ceased
- 1991-03-18 ZA ZA911979A patent/ZA911979B/xx unknown
- 1991-03-18 KR KR1019910004236A patent/KR930010581B1/ko not_active Expired - Fee Related
- 1991-03-18 MY MYPI91000438A patent/MY107235A/en unknown
- 1991-03-19 JP JP3130750A patent/JPH04234815A/ja active Pending
1992
- 1992-07-09 AU AU19574/92A patent/AU637745B2/en not_active Ceased

Also Published As

Publication number	Publication date
HU910872D0 (en)	1991-09-30
AU625409B2 (en)	1992-07-09
IL97521A0 (en)	1992-06-21
KR930010581B1 (ko)	1993-10-30
ZA911979B (en)	1992-10-28
PT97061B (pt)	1998-07-31
EP0448253A2 (en)	1991-09-25
EP0448253A3 (en)	1992-04-01
AU7358791A (en)	1991-12-12
JPH04234815A (ja)	1992-08-24
AU1957492A (en)	1992-09-10
US5008283A (en)	1991-04-16
IE910860A1 (en)	1991-09-25
CA2038409C (en)	1995-01-24
AU637745B2 (en)	1993-06-03
HUT60623A (en)	1992-10-28
NZ237451A (en)	1997-02-24
KR910016326A (ko)	1991-11-05
PT97061A (pt)	1991-10-31
SG48397A1 (en)	1998-04-17
MY107235A (en)	1995-10-31

Legal Events

Date	Code	Title
1996-06-18	FF	Patent granted
1997-07-13	KB	Patent renewed
2001-06-14	KB	Patent renewed
2006-01-15	MM9K	Patent not in force due to non-payment of renewal fees

Publication	Publication Date	Title
AU758147B2 (en)	2003-03-13	The use of MMP-13 selective inhibitors for the treatment of osteoarthristis and other MMP-mediated disorders
USH1286H (en)	1994-02-01	Method for treating peripheral atherosclerotic disease employing a cholesterol lowering drug, an ace inhibitor, or a combination thereof
US5008283A (en)	1991-04-16	Use of tenidap to inhibit activation of collagenase and to inhibit the activity of myeloperoxidase
CA2260995A1 (en)	1998-01-29	Method for lowering serum lipid levels employing an mtp inhibitor in combination with another cholesterol lowering drug
IE911431A1 (en)	1991-11-20	Method for preventing, stabilizing or causing regression of atherosclerosis employing a combination of a cholesterol lowering drug and an ace inhibitor
BR9713921A (pt)	2000-03-21	Composto, composição farmacêutica, processo para tógico capaz de ser modulado através da inibição do fator xa
KR0179315B1 (ko)	1999-03-20	알츠하이머병 치료용 약제
AU601325B2 (en)	1990-09-06	3-substituted-2-oxindole-1-carboxamides as inhibitors of interleukin-1 biosynthesis
CA2060789C (en)	1995-10-17	Use of tenidap to reduce total serum cholesterol, ldl cholesterol and triglycerides
AU629109B2 (en)	1992-09-24	Tenidap as an inhibitor of the release of elastage by neutrophils
CA2286341A1 (en)	1998-11-12	Mtp inhibitors and fat soluble vitamin therapeutic combinations to lower serum lipid levels
EP0543855A1 (en)	1993-06-02	Use of aryl hydroxyurea compounds for the treatment of atherosclerosis
EP0373827B1 (en)	1993-10-27	Derivatives of 5-hydroxy and 5-methoxy 2-amino-pyrimidines as inhibitors of interleukin-1 production
CA2027394C (en)	1995-01-03	3-substituted-2-oxindole derivatives as inhibitors of interleukin-1 biosynthesis
US6630502B2 (en)	2003-10-07	Method for preventing, stabilizing or causing regression of atherosclerosis employing a combination of a cholesterol lowering drug and an ace inhibitor
WO2003104189A3 (en)	2005-09-01	4-pyrazol-phenylalanine derivatives as ace-nep inhibitors
WO2003086466A1 (fr)	2003-10-23	Nouveaux promoteurs de l'expression de la thrombomoduline
US5071852A (en)	1991-12-10	Derivatives of 5-hydroxy and 5-methoxy 2-amino-pyrimidines as inhibitors of interleukin-1 production