Israel state records י"ב באדר התשס"ו March 12, 2006
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- 131962 [21][11] חומרי - ביניים 2, 5 - די
- MANNARIC - 1, 4 : 6, 3 - DILACTONE 2, 5 -ETHERS FOR THE SYNTHESIS OF HIV PROTEASE INHIBITORS
- 132163 [21][11] שימוש בקומבינציה של במעכבי ציקלואוקסיג נאז
- 132318 [21][11] אימידזולים מותמרים היעילים לטיפול במחלות דלקתיות
- SUBSTITUTED IMIDAZOLES USEFUL IN THE TREATMENT OF INFLAMMATORY DISEASES, PHARMACEUTICAL COMPOSITIONS COMPRISING THEM AND A METHOD FOR PREPARING SOME OF THEM
- 132366 [21][11] שיטות לזיהוי תרכובות המעכבות פגע סרטני
- 132761 [21][11] צורות גבישיות של 33– אפיכלורו– 33
- CRYSTALLINE FORMS OF 33-EPICHLORO-33-DESOXYASCOMYCIN, THEIR PREPARATION AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM
| [57] A compound of a pharmaceutically acceptable salt thereof of the formula 
where Q is an optionally substituted phenyl, naphthyl, thiophenyl, benzotriazolyl, benzothiazolyl, benzofuranyl, benzimidazolyl, pyrazolyl, thiazolyl, isoxazolyl or oxochromanyl, indanyl or indanoyl, R1 as hydrogen, methyl, ethyl, propyl, hydroxyethyl, methoxyethyl, formyl, acetyl, trifluoroacetyl or methanesulfonyl, R2 as hydrogen or one or more of methyl, ethyl, n-butyl, iso-propyl, iso-butyl, t-butyl, phenyl, methoxy, ethoxy, iso-propoxy, n-butoxy, iodobenzoyl, trifluoromethyl, perfluoroethyl, trifluoromethoxy, trifluoroacetyl, trifluoromethyldiazinyl, methanesulfonyl, n-propylsulfonyl, isopropylsulfonyl, dimethylsulfamoyl; or two groups R2 form a benzene, cyclopentane or cyclopentanone ring; X as hydrogen, chloro, bromo, iodo, fluoro, amino, trifluoroacetylamino; but when X is hydrogen excluding the compounds 7-(3, 4,5-trimethoxybenzamido)-2-methyl-1, 2, 3, 4-tetrahydroisoquinoline, 7-(2-bromobenzamido)-2-methyl-1,2,3,4-tetrahydroisoquinoline, 7-(2-fluorobenzamido)-1, 2, 3, 4-tetrahydroisoquinoline and compounds in which R2 is 2-alkoxy; and when X is halogen excluding the compounds N-(5-iodo-1, 2, 3, 4-tetrahydroisoquinolin -7-yl)-2-methoxy-4- trifluoromethyldiazirinylbenzamide and N-(5-iodo-1,2,3,4-tetrahydroisoquinolin-7-yl)-2-methoxy-5-trifluoromethyldiazirinylbenzamide. __________
[57] Compounds of the formula 
where Z' and Z" are –(CH2)m P wherein each m is independently 0, 1 or 2 and each P is independently a substituted or unsubsituted member selected from the group consisting of phenyl, cyloexenyl, cyclopentyl, cyclohexanyl, cylopentanyl, indanyl, naphthyl, furyl, thienyl, pyrrolyl, pyrrolinyl, pyrrolidinyl, pyrazolyl, pyrazolinyl, pyrazolidinyl, imidazolyl, imidazolinyl, imidazolidinyl, pyridyl, piperidinyl, pyrazinyl, piperazinyl, primidinyl, pyridazinyl, oxazolyl, oxazlidinyl, isoxazolyl, isoxazolidinyl, morpholinyl, thiazolyl, thiazolidinyl, isothiazolyl, isothiazolidinyl, and bicyclic rings.
____________
[57] A pharmaceutical composition for preventing an inflammation related cardiovascular disorder in a subject comprising a therapeutically effective amount of a compound selected from 5,5-dimethyl-4-(4-methylsulfonyl)phenyl)-3-(2-propoxy)-5H-furan-2-one, 5-methanesulphonamide-6-(2,4-difluorothiophenyl)-1-indanone; and a compound of Formula I comprising a sulfonylphenyl group as shown below 
wherein A is a substituent selected from partially unsaturated or unsaturated heterocyclyl and partially unsaturated or unsaturated carbocyclic rings; wherein R1 is at least one substituent selected from heterocyclyl, cyloalkyl, cycloalkenyl and aryl, wherein R1 is optionally substituted at a substitutable position with one or more radicals selected from alkyl, haloalkyl, cyano, carboxyl, alkoxycarbonyl, hydroxyl, hydroxyalkyl, haloalkoxy, amino, alkylamino, arylamino, nitro, alkoyalkyl, alkylsulfinyl, halo, alkoxy and alkylthio; wherein R2 is methyl or amino; and wherein R3 is one or more radical selected from hydrogen, halo, alkyl, alkenyl, alkynyl, oxo, cyano, carboxyl, cyanoalkyl, heterocyclyloxy, alkyloxy, alkylthio, alkylcarbonyl, cycloalkyl, aryl, haloalkyl, heterocyclyl, cycloalkenyl, aralkyl, heterocyclylalkyl, acyl, alkylthioalkyl, hydroxyalkyl, alkoxycarbonyl, arylcarbonyl, aralkylcarbonyl, aralkenyl, alkoxyalkyl, arylthioalkyl, aryloxyalkyl, aralkylthioalkyl, aralkoxyalkyl, alkoxyaralkoxyalkyl, alkoxycarbonylalkyl, aminocarbonyl, aminocarbonylalkyl, alkylaminocarbonyl, N-arylaminocarbonyl, N-alkyl-N-arylaminocarbonyl, alkylaminocarbonylalkyl, carboxyalkyl, N-arylamino, N-aralkylamino, N-alkyl-N-aralkylamino, N-alkyl-N-arylamino, aminoalkyl, N-arylaminoalkyl, N-aralkylaminoalkyl, N-alkyl-N-aralkylaminoalkyl, N-alkyl-N-arylaminoalkyl, aryloxy, aralkoxy, arylthio, aralkylthio, alkylsulfinyl, alkylsulfonyl, aminosulfonyl, alkylaminosulfonyl, N-arylaminosulfonyl, arylsulfonyl, N-alkyl-N-arylaminosulfonyl; or a pharmaceutically-acceptable salt thereof; provided that if A is imidazole, the sulfonylphenyl group is on the nitrogen atom that is the third ring atom; and that if A is pyrazole the sulfonylphenyl group is not substituted on a pyrazole ring nitrogen atom or the pyrazole ring carbon atom which is the fifth ring atom; and that if A is oxazole, the sulfonylphenyl group is not substituted on the oxazole ring carbon atom that is the fifth ring atom; and that if A is isoxazole, the sulfonylphenyl group is not substituted on the isoxazole ring carbon atom that is the third or fourth ring atom; and that if A is thiazole, the sulfonylphenyl group is not substituted on the thiazole ring carbon atom that is the fourth or fifth ring atom; for manufacture of a pharmaceutical composition for preventing an inflammation related cardiovascular disorder in a subject, provided the pharmaceutical composition is not in combination with a 5-lipoxygenase inhibitor, a leukotriene-A4- hydrolase inhibitor, or a leukotriene-B4-receptor antagonist, wherein the cardiovascular disorder is selected from prevention of coronary artery disease, aneurysm, embolism, angina including unstable angina, coronary plaque inflammation, bacterial-induced inflammation including Chlamydia-induced inflammation, and inflammation associated with surgical procedures such as vascular grafting including coronary artery bypass surgery, revascularization procedures including angioplasty, stent placement, endarterectomy and other invasive procedures involving arteries, veins and capillaries. __________
[57] A compound of the formula 
wherein: R1 is phenyl, substituted phenyl (wherein each substituent is C1-5 alkyl, halogen, nitro, trifluoromethyl or nitrile) or heteroaryl wherein the heteroaryl contains 6 ring atoms and contains up to three nitrogen atoms as heteroatoms; R2 is phenyl, substituted phenyl (wherein each subsitutent is C1-5 alkyl, halogen, nitro, trifluoromethyl or nitrile), heteroaryl wherein the heteroaryl contains 6 ring atoms and contains up to three nitrogen atoms as heteroatoms and is optionally C1-4 alkyl substituted; R3 is hydrogen, SEM C1-5 alkoycarbonyl, aryloxycarbonyl, aryl C1-5 alkyloxycarbonyl, aryl C1-5 alkyl, substituted aryl C1-5 alkyl (wherein each aryl subsituent is independently C1-5 alkyl, C1-5 alkoxy, halogen, amino, C1-5 alkylamino or di C1-5 alkylamino), phthalimido-C1-5 alkyl, amino C1-5 alkyl, diamino C1-5 alkyl, succinimido C1-5 alkyl, C1-5 alkylcarbonyl, arylcarbonyl, C1-5 alkylcarbonyl C1-5 alkyl, aryloxycarbonyl C1-5 alkyl or heteroaryl C1-5 alkyl wherein the heteroaryl contains 6 ring atoms and contains up to three nitrogen atoms as heteroatoms; R4 is (A)-(CH2)q-X; A is vinylene, ethynylene or 
R5 is hydrogen, C1-5 alkyl, phenyl or phenyl C1-5 alkyl; q is 0-9; X is hydrogen, hydroxy, vinyl, substituted vinyl (wherein each subsituent is fluorine, bromine, chlorine or iodine), ethynyl, substituted ethynyl (wherein each subsituent is fluorine, bromine, chlorine or iodine), C1-5 alkyl, substituted C1-5 alkyl (wherein each alkyl substituent is C1-5 alkoxy, trihalo C1-5 alkyl, phthalimido or amino) C3-7 cycloalkyl, C1-5 alkoxy, substituted C1-5 alkoxy (wherein each alkyl substituent is phthalimido or amino), phthalimidoxy, phenoxy, substituted phenoxy (wherein each phenyl substituent is C1-5 alkyl, halogen or C1-5 alkoxy), phenyl, substituted phenyl (wherein each phenyl substituent is C1-5 alkyl, halogen or C1-5 alkoxy), aryl C1-5 alkyl, substituted aryl C1-5 alkyl wherein each aryl substituent is C1-5 alkyl, halogen or C1-5 alkoxy), arylhydroxy C1-5 alkyl amino, C1-5 alkylamino, di C1-5 alkylamino, nitrile, oxime, benzyloxyimino, C1-5 alkyloxyimino, phthalimido, succinimido, C1-5 alkycarbonyloxy, phenylcarbonyloxy, substituted phenylcarbonyloxy (wherein each phenyl substituent is C1-5 alkyl, halogen or C1-5 alkyl, halogen or C1-5 alkoxy), phenyl C1-5 alkylcarbonyloxy (wherein each phenyl substituent is (C1-5 alkyl, halogen or C1-5 alkoxy), aminocarbonyloxy, C1-5 alylaminocarbonyloxy, diC1-5 alkylaminocarbonyloxy, C1-5 alkoxycarbonyloxy, substituted C1-5 alkoycarbonyloxy (wherein each alkyl substituent is methyl, ethyl, isopropyl or hexyl), phenoxycarbonyloxy, substituted phenoxycarbonyloxy (wherein each phenyl substituent is C1-5 alkyl, C1-5 alkoxy or halogen), C1-5 alkylthio, substituted C1-5 alkylthio (wherein each alkyl substituent is hydroxy or phthalimido), C1-5 alkylsulfonyl, phenylsulfonyl, substituted phenylosulfonyl (wherein each phenyl substituent is bromine, fluorine, chlorine, C1-5 alkoxy or trifluoromethyl); with the proviso: if A is
q is 0 and X is H, R3 may not be SEM; and pharmaceutically acceptable salts thereof. __________
[57] A method for selecting a compound for the treatment of neoplasia, comprising: determining the cyclooxygenase (COX) inhibitory activity of the compound; determining the PDE2 inhibition activity of the compound; and selecting the compound that has COX inhibitory activity lower than said PDE activity for treating neoplasia. __________
Directory: Units -> RashamHaptentim -> Units -> patent -> yoman Units -> Perform and explain geodetic computations Units -> Demonstrate and apply advanced knowledge of programming techniques for electrotechnology Units -> Nzqa registered unit standard 22561 version 3 Units -> Nzqa registered unit standard 22528 version 2 Units -> Nzqa registered unit standard 26968 version 1 Units -> Nzqa registered unit standard 10212 version 5 Download 0.86 Mb. Share with your friends:
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