Clarion Pharmaceuticals Inc.

Other

Chemie Linz Aktiengesellschaft

Austria Wirtschaftsservice Gesellschaft MIT Beschrankter Haftung

Cl Pharma Aktiengesellschaft

Hafslund Nycomed Pharma Aktiengesellschaft

Technische Universitat Graz

Forschungsholding Tu Graz Gmbh

Albin Hermetter

Friedrich Paltauf

Rudolf Franzmair

Peter Langen

Olga Oskolkova

Haridasan K Nair

Andrew C Peterson

Christine Lehmann

Iduna Fichtner

Reinhild Schonfeld

Hans Brachwitz

Eckart Matthes

Michael Trenker

Jurgen Schildt

The invention relates to oxidized phospholipids having one of the general formulas (I) or (II) wherein A&#x2550;O, C, NH, or S; B&#x2550;O, C, NH, or S; and Ris selected from the group consisting of &#x2014;CO&#x2014;(CH)&#x2014;CH; &#x2014;CO&#x2014;(CH)&#x2014;CHO; and &#x2014;CO&#x2014;(CH)&#x2014;COOH, with n=3-7, with the proviso that in general formula (I), Ris selected from the group consisting of &#x2014;CH&#x2014;(CH)&#x2014;X; and &#x2014;CO&#x2014;(CH)&#x2014;X with n=5-11, wherein X is a fluorophore; and in general formula (II), Ris selected from the group consisting of &#x2014;CH&#x2550;CH&#x2014;(CH)&#x2014;CHwith n=9-15; &#x2014;(CH)&#x2014;CHwith n=11-17; and &#x2014;CO&#x2014;(CH)&#x2014;CHwith n=10&#x2014;16; and Ris selected from the group consisting of &#x2014;CO&#x2014;(CH)&#x2014;X; and &#x2014;SO&#x2014;(CH)&#x2014;X, with n=0-5, wherein X is a fluorophore. 

Oxidized phospholipids

The invention relates to compounds having general formula I in which X represents an optically detectable moiety, n is an integer with 1&#x2266;n&#x2266;20, Ris an unbranched or branched alkyl group having 1 to 20 carbon atoms, and Ris hydrogen or &#x2014;CH&#x2014;O&#x2014;Rgroup, wherein Rhas the same meaning as R. These compounds are useful as inhibitors of lipolytic enzymes and can be used as tools for analysis as well as discrimination of lipolytic enzymes in biological samples.

Optically detectable organophosphonates

Heteroaryl-substituted deoxy glycerols represented by the general Formulas Ia, Ib and Ic: ##STR1## wherein: X is oxygen (--O--) or sulfur (--S--); R is substituted or unsubstituted straight or branched chain C.sub.1-30 alkyl or alkenyl, provided that a double bond of the alkenyl does not originate at the carbon atom bound to the X substituent; Het is a 5- to 9-membered heteroaryl mono- or bicyclic ring system having no more than 1 carbonyl carbon in the ring system, with 1 to 4 nitrogen atoms as the sole heteroatoms, one of which nitrogens is bonded to the glycero carbon; and Y is hydroxyl (--OH) or thiol (--SH), pharmaceutical compositions containing the same, and methods of using the compounds, are disclosed. The compounds exhibit antiviral and antibacterial activities.

Heteroaryl-substituted deoxy glycerols and antibacterial and antiviral

Therapeutically active, heteroaryl-substituted deoxy glycero-phosphoethanolamines are disclosed having the general Formula I: ##STR1## wherein one of X, Y or Z is a fatty ether substituent, one is a heteroaryl ring substituent with 1-4 nitrogens as the only heteroatoms, one of which is bonded to a carbon of the glyceryl backbone, and one is a phosphoethanolamine substituent substituted at the nitrogen, provided that each of X, Y and Z is a different substituent, and the pharmaceutical compositions comprising the therapeutically active compounds and methods of using the therapetically active compounds to treat cancerous tumors, psoriasis and inflammation are also disclosed.

Heteroaryl-substituted deoxy glycero-phosphoethanolamines

The present invention relates to novel, therapeutically active fatty alkyl and alkenyl ether glycerophospholipids bearing a 3-(2-imidazolinyl)-2-imidazolinyl or 2-imidazolinyl substituent on the ethanolamine nitrogen, methods of using the compounds and pharmaceutically acceptable salts thereof, and pharmaceutical compositions containing same. The novel, therapeutically active compounds and salts of the invention possess anti-tumor, anti-psoriatic, anti-inflammatory, and anti-asthma activities.

N-substituted glycerophosphoethanolamines

Alkylphosphonoserines and pharmaceutical compositions useful as

The invention relates to novel glycero-3(2)phospho-L-serine derivatives of the general formula ##STR1## in which A represents unsubstituted or substituted (C5-C30) alkoxy, or unsubstituted or substituted (C5-C30) alkenoxy, whereby a double bond of the alkenoxy residue does not originate at the C atom bound to oxygen, or halogen, or a group of the general formula

Glycero-3(2)-phospho-L-serine derivatives and salts thereof

Single-stage process for preparing mixed-substituted enantiomerically pure 1,2-diacyl-sn-glycero-3-phosphocholines of general formula I ##STR1## in which R.sub.1 and R.sub.2 are different and independently of each other denote a substituted or unsubstituted C.sub.1 to C.sub.24 -alkyl or C.sub.3 to C.sub.24 -alkenyl radical, by reacting 1-0-triphenylmethyl-2-acyl-sn-glycero-3-phosphocholine of the general formula ##STR2## in which T denotes a substituted or unsubstituted triphenylmethyl group and R.sub.2 is as defined above, with a reactive carboxylic acid derivative of the general formula

Single-stage process for preparing mixed-substituted

Preparation of chemically defined pure enantiomeric 1,2-diacyl-sn-glycero-3-phosphocholines and 1,2-diacyl-sn-glycero-3-phosphoethanolamines which are substituted in positions 1 and 2 of the glycerol, by acylation of triphenylmethyl derivatives of sn-glycero-3-phosphocholine and sn-glycero-3-phosphoethanolamine.

Preparation of acylated glycerophosphocholines and

The invention relates to new triphenylmethyl derivatives of sn-glycero-3-phosphocholine and sn-glycero-3-phosphoethanolamine of the general formula ##STR1## in which T denotes a triphenylmethyl group which is unsubstituted or monosubstituted or polysubstituted by C.sub.1 -C.sub.6 -alkyl, C.sub.1 -C.sub.6 -alkoxy or halogen, and the radicals R.sub.1, R.sub.2 and R.sub.3 either are identical and each represent a methyl group, or are different, in which case two of the radicals R.sub.1, R.sub.2 and R.sub.3 always denote hydrogen, and the third radical represents a triphenylmethyl group which is unsubstituted or monosubstituted or polysubstituted by C.sub.1 -C.sub.6 -alkyl, C.sub.1 -C.sub.6 -alkoxy or halogen,

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Graz, Austria

Albin Hermetter