Syntex (u.s.a.) Inc.

John J Nestor, Jr

Brian H Vickery

John L Krstenansky

Teresa H Ho

Chinh T Bach

Gordon H Jones

Hans Maag

John G Moffatt

Milan R Uskokovic

John O Link

Philip L Felgner

Percy Sarwood Manchand

Humberto Bartolome Arzeno

Gary A Peltz

Deborah A Eppstein

Paula Nanette Belloni

Donald Roy Hirschfeld

Scott William Womble

Natalie L McClure

Barbara P Barna

Sharad D Deodhar

Synthetic polypeptide analogs of parathyroid hormone PTH, parathyroid hormone related peptide PTHrp, and of the physiologically active truncated homologs and analogs of PTH and PTHrp, in which amino acid residues (22-31) form an amphipathic .alpha.-helix, said residues (22-31) selected from hydrophilic amino acids (Haa) and lipophilic amino acids (Laa) ordered in the sequence:

Analogs of parathyroid hormone and parathyroid hormone related peptide:

This invention provides novel cationic lipids, particularly guanidino lipids, and methods for their preparation. Also provided are polyanionic-lipid complexes comprising the lipids of the invention, their preparation and use to deliver biologically active substances, particularly nucleic acids to cells.

Cationic lipids for gene therapy

Synthesis and use for the treatment of osteoporosis

Fluorinated Vitamin D.sub.3 analogs, intermediates for their preparation, compositions comprising the analogs and methods of treatment of osteoporosis and related conditions with these and related analogs are provided.

Fluorinated vitamin D3 analogs

The L-monovaline ester derived from 2-(2-amino-1,6-dihydro-6-oxo-purin-9-yl)methoxy-1,3-propanediol and its pharmaceutically acceptable salts are of value as antiviral agents with improved absorption.

2-(2-amino-1,6-dihydro-6-oxo-purin-9-yl) methoxy-1,3-propanediol

Analogs of parathyroid hormone and parathyroid hormone relate peptide

Process for recombinant production of PTH and PTHrp analogs

Compounds having immunomodulatory activity comprising the optionally modified dodecapeptide fragment A-(SEQ ID No: 1)-B corresponding to residues 174 to 185 of C-reactive protein (CRP), pharmaceutical compositions thereof, and methods of treating cancer with the compositions. Liposomal formulations containing the CRP-peptide fragment are particularly efficacious when administered in conjunction with interleukin-2.

C-reactive protein fragment with immunomodulatory activity

Synthetic nona- and decapeptide LHRH antagonist analogs are disclosed, having a sterically hindered guanidino-substituted arginyl or homoarginyl residue at position 8, with no arginyl substituent at position 6.

Nonapeptide and decapeptide analogs of LHRH useful as LHRH antagonists

Synthetic polypeptide analogs of parathyroid hormone PTH, parathyroid hormone related peptide PTHrp, and of the physiologically active truncated homologs and analogs of PTH and PTHrp, in which amino acid residues (22-31) form an amphipathic .alpha.-helix, these residues (22-31) selected from hydrophilic amino acids (Haa) and lipophilic amino acids (Laa) ordered in the sequence:

Compounds of the Formula I ##STR1## wherein X is hydrogen, chloro, amino or hydroxy; R.sup.1 is an achiral amino acid acyl residue with a tertiary .alpha.-carbon atom. Preferred achiral amino acid acyl residues have the formula ##STR2## wherein each R.sup.2 is alkyl with 1 to 6 carbon atoms, cycloalkyl with 3 to 5 carbon atoms, or benzyl; or the two R.sup.2 groups link together to form a polymethylene group with 3 to 9 carbon atoms, and pharmaceutically acceptable salts thereof are antiviral agents with improved absorption. Intermediates for the preparation of the compounds of Formula I are also described.

Achiral amino acid acyl esters of ganciclovir and its derivatives

In a process for the solid phase synthesis of a polypeptide containing at least one serine residue, the improvement comprising temporarily protecting the side chain of the serine residue with a protecting group which is removed immediately following the addition of the serine to the peptide chain.

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Cupertino, CA, United States of America

John J Nestor, Jr