HUP0204131A2 - Saccharin derivatives as orally active elastase inhibitors, process for their preparation and pharmaceutical compositions containing them - Google Patents
Saccharin derivatives as orally active elastase inhibitors, process for their preparation and pharmaceutical compositions containing themInfo
- Publication number
- HUP0204131A2 HUP0204131A2 HU0204131A HUP0204131A HUP0204131A2 HU P0204131 A2 HUP0204131 A2 HU P0204131A2 HU 0204131 A HU0204131 A HU 0204131A HU P0204131 A HUP0204131 A HU P0204131A HU P0204131 A2 HUP0204131 A2 HU P0204131A2
- Authority
- HU
- Hungary
- Prior art keywords
- general
- new
- saccharin derivatives
- preparation
- antipsoriatic
- Prior art date
Links
- CVHZOJJKTDOEJC-UHFFFAOYSA-N saccharin Chemical class C1=CC=C2C(=O)NS(=O)(=O)C2=C1 CVHZOJJKTDOEJC-UHFFFAOYSA-N 0.000 title abstract 3
- 239000003602 elastase inhibitor Substances 0.000 title abstract 2
- 239000008194 pharmaceutical composition Substances 0.000 title 1
- -1 2-morpholino-ethyl Chemical group 0.000 abstract 2
- 101000851058 Homo sapiens Neutrophil elastase Proteins 0.000 abstract 2
- 230000002682 anti-psoriatic effect Effects 0.000 abstract 2
- 230000005764 inhibitory process Effects 0.000 abstract 2
- DRZXDZYWZSKFDL-UHFFFAOYSA-N 6-methoxy-1,1-dioxo-2-[[4-oxo-9-[2-(1-piperidinyl)ethoxy]-2-pyrido[1,2-a]pyrimidinyl]oxymethyl]-4-propan-2-yl-1,2-benzothiazol-3-one Chemical compound CC(C)C1=CC(OC)=CC(S2(=O)=O)=C1C(=O)N2COC(N=C12)=CC(=O)N1C=CC=C2OCCN1CCCCC1 DRZXDZYWZSKFDL-UHFFFAOYSA-N 0.000 abstract 1
- 229940122858 Elastase inhibitor Drugs 0.000 abstract 1
- 208000001953 Hypotension Diseases 0.000 abstract 1
- 241001465754 Metazoa Species 0.000 abstract 1
- 241000699670 Mus sp. Species 0.000 abstract 1
- 230000001154 acute effect Effects 0.000 abstract 1
- 230000003266 anti-allergic effect Effects 0.000 abstract 1
- 230000002456 anti-arthritic effect Effects 0.000 abstract 1
- 230000001088 anti-asthma Effects 0.000 abstract 1
- 230000000844 anti-bacterial effect Effects 0.000 abstract 1
- 230000003110 anti-inflammatory effect Effects 0.000 abstract 1
- 230000003356 anti-rheumatic effect Effects 0.000 abstract 1
- 230000000767 anti-ulcer Effects 0.000 abstract 1
- 239000000924 antiasthmatic agent Substances 0.000 abstract 1
- 239000003435 antirheumatic agent Substances 0.000 abstract 1
- 150000001875 compounds Chemical class 0.000 abstract 1
- 239000000824 cytostatic agent Substances 0.000 abstract 1
- 230000001085 cytostatic effect Effects 0.000 abstract 1
- 230000000254 damaging effect Effects 0.000 abstract 1
- 230000000694 effects Effects 0.000 abstract 1
- 230000002124 endocrine Effects 0.000 abstract 1
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 abstract 1
- 239000012530 fluid Substances 0.000 abstract 1
- 230000002496 gastric effect Effects 0.000 abstract 1
- 230000002008 hemorrhagic effect Effects 0.000 abstract 1
- 230000001553 hepatotropic effect Effects 0.000 abstract 1
- 150000004677 hydrates Chemical class 0.000 abstract 1
- 208000021822 hypotensive Diseases 0.000 abstract 1
- 230000001077 hypotensive effect Effects 0.000 abstract 1
- 230000001506 immunosuppresive effect Effects 0.000 abstract 1
- 239000000543 intermediate Substances 0.000 abstract 1
- 210000004072 lung Anatomy 0.000 abstract 1
- 230000010534 mechanism of action Effects 0.000 abstract 1
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 abstract 1
- 125000004573 morpholin-4-yl group Chemical group N1(CCOCC1)* 0.000 abstract 1
- 230000000324 neuroprotective effect Effects 0.000 abstract 1
- 239000002504 physiological saline solution Substances 0.000 abstract 1
- 125000000587 piperidin-1-yl group Chemical group [H]C1([H])N(*)C([H])([H])C([H])([H])C([H])([H])C1([H])[H] 0.000 abstract 1
- 230000000241 respiratory effect Effects 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 239000012453 solvate Substances 0.000 abstract 1
- 229940125725 tranquilizer Drugs 0.000 abstract 1
- 239000003204 tranquilizing agent Substances 0.000 abstract 1
- 230000002936 tranquilizing effect Effects 0.000 abstract 1
- 239000012873 virucide Substances 0.000 abstract 1
Landscapes
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
Abstract
Saccharin derivatives (I), are new. Saccharin derivatives of formula (I) and their salts, solvates and hydrates are new. [Image] R1>methyl, ethyl or 2-morpholino-ethyl; R2>piperidino, morpholino or 4 methyl-piperazinyl; n : 2 or 3. Independent claims are included for: (a) preparation of (I); and (b) new intermediates of formula (III). [Image] ACTIVITY : Antiasthmatic; Antirheumatic; Antiarthritic; Antiinflammatory; Cytostatic; Antiulcer; Antiallergic; Hepatotropic; Virucide; Dermatological; Immunosuppressive; Nephrotropic; Antipsoriatic; Neuroprotective; Antibacterial; Cardiant; Tranquilizer; Vulnerary; Respiratory General; Antipsoriatic. Hypotensive; Gastrointestinal General; Endocrinal General. MECHANISM OF ACTION : Elastase inhibitor. A test was carried out to determine inhibition of acute lung damaging effect caused by human leukocyte elastase enzyme in mice. Test compounds were administered per os, and 1 hour later, human leukocyte elastase enzyme in physiological saline solution was administered intratracheally. After 3 hours the animals were euthanized. Bronchoalveolar lavage fluids were examined and haemorrhagic response determined. 2-(9-(2-Piperidino-ethoxy)-4 oxo-4H-pyrido(1,2-a)pyrimidin-2-yl-oxymethyl)-4-isopropyl-6 methoxy-1,2-benzisothiazol-3(2H)-one-1,1-dioxide (Ia) at 10 mg/kg showed 80 % inhibition.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| HU0204131A HUP0204131A2 (en) | 1999-12-17 | 2000-12-14 | Saccharin derivatives as orally active elastase inhibitors, process for their preparation and pharmaceutical compositions containing them |
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| HU9904624A HUP9904624A2 (en) | 1999-12-17 | 1999-12-17 | Saccharin derivatives, process for producing them, pharmaceutical compositions containing the same and intermediates |
| PCT/HU2000/000130 WO2001044245A1 (en) | 1999-12-17 | 2000-12-14 | Saccharin derivatives as orally active elastase inhibitors |
| HU0204131A HUP0204131A2 (en) | 1999-12-17 | 2000-12-14 | Saccharin derivatives as orally active elastase inhibitors, process for their preparation and pharmaceutical compositions containing them |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| HUP0204131A2 true HUP0204131A2 (en) | 2003-04-28 |
Family
ID=89980962
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| HU0204131A HUP0204131A2 (en) | 1999-12-17 | 2000-12-14 | Saccharin derivatives as orally active elastase inhibitors, process for their preparation and pharmaceutical compositions containing them |
Country Status (1)
| Country | Link |
|---|---|
| HU (1) | HUP0204131A2 (en) |
-
2000
- 2000-12-14 HU HU0204131A patent/HUP0204131A2/en unknown
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