NO933596L - NEW 2-SPIROCYCLOPROPYLECEPHALOSPORINE SULFON DERIVATIVES AND THEIR PREPARATION - Google Patents
NEW 2-SPIROCYCLOPROPYLECEPHALOSPORINE SULFON DERIVATIVES AND THEIR PREPARATIONInfo
- Publication number
- NO933596L NO933596L NO93933596A NO933596A NO933596L NO 933596 L NO933596 L NO 933596L NO 93933596 A NO93933596 A NO 93933596A NO 933596 A NO933596 A NO 933596A NO 933596 L NO933596 L NO 933596L
- Authority
- NO
- Norway
- Prior art keywords
- alkyl
- substituted
- ring
- phenyl
- optionally substituted
- Prior art date
Links
- RAHZWNYVWXNFOC-UHFFFAOYSA-N Sulphur dioxide Chemical class O=S=O RAHZWNYVWXNFOC-UHFFFAOYSA-N 0.000 title 1
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 abstract 5
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 abstract 4
- -1 sulfone compound Chemical class 0.000 abstract 3
- 125000003545 alkoxy group Chemical group 0.000 abstract 2
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 abstract 2
- 150000001875 compounds Chemical class 0.000 abstract 2
- 229910052739 hydrogen Inorganic materials 0.000 abstract 2
- 239000001257 hydrogen Substances 0.000 abstract 2
- 229910052757 nitrogen Inorganic materials 0.000 abstract 2
- 125000004433 nitrogen atom Chemical group N* 0.000 abstract 2
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 abstract 1
- 241000124008 Mammalia Species 0.000 abstract 1
- 102000016387 Pancreatic elastase Human genes 0.000 abstract 1
- 108010067372 Pancreatic elastase Proteins 0.000 abstract 1
- 125000005092 alkenyloxycarbonyl group Chemical group 0.000 abstract 1
- 125000004453 alkoxycarbonyl group Chemical group 0.000 abstract 1
- 125000000217 alkyl group Chemical group 0.000 abstract 1
- 125000003917 carbamoyl group Chemical class [H]N([H])C(*)=O 0.000 abstract 1
- 229910052799 carbon Inorganic materials 0.000 abstract 1
- 125000004432 carbon atom Chemical group C* 0.000 abstract 1
- 230000003412 degenerative effect Effects 0.000 abstract 1
- 125000000623 heterocyclic group Chemical group 0.000 abstract 1
- 150000002431 hydrogen Chemical class 0.000 abstract 1
- 230000002757 inflammatory effect Effects 0.000 abstract 1
- 230000001404 mediated effect Effects 0.000 abstract 1
- 230000001575 pathological effect Effects 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 230000001225 therapeutic effect Effects 0.000 abstract 1
- 125000001425 triazolyl group Chemical group 0.000 abstract 1
Landscapes
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
Abstract
2-spirocyklopropylcefalosporlnsulfonforbindelsermed formelen: der R1 er OR6 eller NR7R8; R2 er en C- ,-alkylgruppe som kan være substituert med en triazolylgruppe; R3 er fenyl; R4 er fenyl; R5 er en Cj.-alkoksygruppe; R(, er hydrogen, eventuelt substituert -CH2-fenyl eller eventuelt substituert -CH(fenyl )2, der fenylgruppene kan være substituert med minst en C1_,-alkoksygruppe; R7 er C. ,-alkyl som kan være substituert med 1-2 COOH eller C- 7-alkoksykarbonyl, eventuelt substituert tlazolyl, eller R7 sammen med Rg kan danne en eventuelt substituert ring der ringen kan være substituert med minst en av C^-alkyl, hydroksy-C^-alkyl. -COQH, C^-alkyl-COOH, C2_7-alkoksykarbonyl, C^-alkoksy- karbonyl-C ,-alkyl, karboksamid som kan være substituert med (^ ,-alkyl-COOH eller Cjj^-alkoksykarbonyl- C1_6-alkyl, heterocykllsk ring som kan være substituert med C^-alkyl, COOH eller C-, -alkenyloksykarbonyl, og ringen kan inneholde minst et annet nltrogenatom, i hvilket tilfelle ringen ytterligere kan være substi- tuert på karbonatomet eller på nitrogenatoniet med de ovenfor nevnte grupper; Rg er hydrogen eller sammen med R7 danner en eventuelt substituert ring som angitt ovenfor; eller et farmasaytlsk eller et veterlnærmedisinsk akseptabelt salt derav. Forbindelsene med formel (I) rapporteres å ha interessante terapeutiske egenskaper for kontroll av inflanuiato- riske eller degenerative tilstander, særlig elastase-medlerte patologiske tilstander, hos pattedyr. COR. Forbindelsenes fremstilling beskrives.2-spirocyclopropylcephalosporin sulfone compound having the formula: wherein R 1 is OR 6 or NR 7 R 8; R2 is a C1-6 alkyl group which may be substituted by a triazolyl group; R3 is phenyl; R 4 is phenyl; R 5 is a C 1-4 alkoxy group; R 1, is hydrogen, optionally substituted -CH 2 -phenyl or optionally substituted -CH (phenyl) 2, wherein the phenyl groups may be substituted by at least one C 1-4 alkoxy group; R 7 is C COOH or C7-alkoxycarbonyl, optionally substituted tlazolyl, or R7 together with R8 may form an optionally substituted ring wherein the ring may be substituted by at least one of C1-6 alkyl, hydroxy-C1-6 alkyl. alkyl COOH, C2-7 alkoxycarbonyl, C1-6 alkoxycarbonyl-C1-6 alkyl, carboxamide which may be substituted by (C1-6 alkyl COOH or C1-6 alkoxycarbonyl-C1-6 alkyl, heterocyclic ring which may be substituted C 1-6 alkyl, COOH or C 1-6 alkenyloxycarbonyl, and the ring may contain at least one other nitrogen atom, in which case the ring may be further substituted on the carbon atom or on the nitrogen atom by the above groups; R 8 is hydrogen or together with R 7 forms an optionally substituted ring as indicated above, or a pharmaceutical or a veterinarily acceptable salt thereof. The compounds of formula (I) are reported to have interesting therapeutic properties for the control of inflammatory or degenerative conditions, especially elastase-mediated pathological conditions, in mammals. COR. The preparation of the compounds is described.
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US07/685,960 US5264430A (en) | 1989-10-06 | 1991-04-08 | 2-spirocyclopropyl cephalosporin sulfone derivatives |
| US07/747,762 US5264429A (en) | 1989-10-06 | 1991-08-20 | 2-spirocyclopropyl cephalosporin sulfone derivatives |
| PCT/CA1992/000146 WO1992018474A2 (en) | 1991-04-08 | 1992-04-07 | Novel 2-spirocyclopropyl cephalosporin sulfone derivatives and processes for the preparation thereof |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| NO933596D0 NO933596D0 (en) | 1993-10-07 |
| NO933596L true NO933596L (en) | 1993-10-07 |
Family
ID=27171659
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| NO93933596A NO933596L (en) | 1991-04-08 | 1993-10-07 | NEW 2-SPIROCYCLOPROPYLECEPHALOSPORINE SULFON DERIVATIVES AND THEIR PREPARATION |
Country Status (1)
| Country | Link |
|---|---|
| NO (1) | NO933596L (en) |
-
1993
- 1993-10-07 NO NO93933596A patent/NO933596L/en unknown
Also Published As
| Publication number | Publication date |
|---|---|
| NO933596D0 (en) | 1993-10-07 |
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