American Cyanamid Company

Innapharma, Inc.

Wyeth Holdings Corporation

Collagenex Pharmaceuticals, Incorporated

Other

Galderma Laboratories Inc.

Tetragenex Pharmaceuticals, Inc.

Joseph J Hlavka

Panayota Bitha

Yang-I Lin

Phaik-Eng Sum

Ving J Lee

Ralph G Child

Raymond T Testa

Yakov Gluzman

Henry B Abajian

John Fowler Noble

Adma A Ross

Robert A Ashley

Andrew S Kende

Matthew R Pincus

Yang I Lin

Richard J Ablin

John P Feighner

The present invention provides new chemically modified 4-dedimethylaminotetracycline compounds that can be substituted with aryl, alkenyl, or alkynyl groups. The 7, 8, and/or 9 positions and methods for preparing such compounds. Other tetracycline compounds include the 4-dedimethylaminotetracycline derivatives with an oxime group, NH-Alkyl, or N&#x2014;NH-Alkyl group substituted at the C4 position as well as C2 Mannich derivatives. The present invention also provides a method of treating a mammal suffering from conditions or diseases by administering to the mammal an effective amount of the new chemically modified tetracycline compounds.

4-dedimethylaminotetracycline derivatives

The invention is drawn to 7-substituted-9-(substituted amino)-6-demethyl-6-deoxytetracycline compounds of the formulawherein R, X, Rand Rare defined in the specification. The compounds of the invention are useful as broad spectrum antibiotics.

7-Substituted-9-substituted amino-6-demethyl-6-deoxytetracyclines

The disclosure is drawn to a method of using novel 7-substituted-9-(substituted amino)-6-demethyl-6-deoxytetracycline compounds to treat infections caused by a wide spectrum of bacterial organisms, including those which are resistant to tetracycline.

Method for treating bacterial infection with novel 7-substituted-9-substituted amino 6-demethyl-6-deoxytetracyclines

A treatment for inhibiting microbial or tumor growth is disclosed, which comprises adding to a subject in need of treatment an effective amount of one or more tetracycline derivatives.

Tetracycline derivatives and methods of use thereof

Novel uses of certain peptides to treat patients suffering from neurological or psychiatric disorders are disclosed. The peptides include the tripeptide hormone MIF and compounds made by modifications of MIF, such as modification of amino terminus residues, carboxyl terminus residues and internal residues, including addition and substitution of amino acid residues and modification of the peptide bonds and functional side groups of respective amino acid residues. The tri-, tetra-, penta-, peptides and polypeptides may be utilized alone or in combination with other agents, to treat patients suffering from physiological, psychosomatic, neurological or psychiatric disorders.

Therapeutic uses of tri-, tetra-, penta-, and polypeptides

The present invention provides new chemically modified 4-dedimethylaminotetracycline compounds that can be substituted with aryl, alkenyl, or alkynyl groups. The 7, 8, and/or 9 positions and methods for preparing such compounds. Other tetracycline compounds include the 4-dedimethylaminotetracycline derivatives with an oxime group, NH-Alkyl, or N&mdash;NH-Alkyl group substituted at the C4 position as well as C2 Mannich derivatives. The present invention also provides a method of treating a mammal suffering from conditions or diseases by administering to the mammal an effective amount of the new chemically modified tetracycline compounds.

The present invention provides new chemically modified 4-dedimethylaminotetracycline compounds that can be substituted at the 7, 8, and/or 9 positions and methods for preparing the 4-dedimethylamino tetracycline compounds. Other tetracycline compounds are the 4-dedimethylaminotetracycline derivatives with an oxime group, NH-Alkyl, or N&mdash;NH-Alkyl group at the C4 position. The present invention also provides a method of treating a mammal suffering from conditions or diseases by administering to the mammal an effective amount of the new chemically modified 4-dedimethylamino tetracycline compounds.

Organic platinum complexes active as anti-tumor agents in warm-blooded animals, and methods for synthesis of same, are described.

(Gem-heterocyclodimethanamine-n,n&prime;)platinum complexes

The present invention discloses novel peptides utilized to treat patients suffering from depression. These novel peptides are modifications of the tripeptide hormone MIF, including modification of amino terminus residues, carboxyl terminus residues and internal residues, including addition and substitution of amino acid residues and modification of the peptide bonds and functional side groups of respective amino acid residues. The tri-, tetra-, penta-, peptides and polypeptides of the present invention may be utilized alone or in combination to treat patients suffering from depression.

Tri-, Tetra-, Penta-, and polypeptides and their therapeutic use as an

This invention provides peptidomimetics which bind to T4 or CD4 cell receptors and are useful in inhibiting viral infectivity by viruses which bind to T4 cell receptors. More specifically, peptidomimetics of this invention can alleviate symptoms of AIDS by inhibiting binding of HIV, the virus associated with AIDS, to receptor sites in human cells susceptible to HIV infection. These peptidomimetics, in particular, inhibit binding of HIV to cells of brain membrane and the immune system. They also display substantially longer half-lives in vivo than peptide T. The compounds of this invention which bind to T4 or CD4 receptors and thereby inhibit binding of HIV, alone or in combination with one another, can be used to alleviate AIDS symptoms and ameliorate symptoms of HIV infection, especially neuronal dementias and Kaposi's sarcoma. The compounds of this invention, alone or in combination, can further be used to prevent development of AIDS in persons who might become exposed to HIV.

Peptidomimetics for the treatment of HIV infection

The present invention provides peptides, cyclized peptides and peptidomimetics which inhibit the oncogenic and/or transforming activity of the p21 ras protein, pharmaceutical compositions containing at least one of the ras-inhibiting peptides, cyclized peptides and peptidomimetics, and methods for inhibiting the ras-mediated oncogenic and/or transformation process in mammalian cells or tissues.

Peptidomimetics inhibiting the oncogenic action of p21 ras

The invention provides compounds of the formulas ##STR1## which are useful as intermediates for the preparation of 6-demethyl-6-deotetracycline antibiotic agents.

7-(substituted)-8-(substituted)-9-(substitued

The present invention provides peptides and cyclized peptides which inhibit the oncogenic and/or transforming activity of the p21 ras protein, pharmaceutical compositions containing at least one of the ras-inhibiting peptides, cyclized peptides and peptidomimetics, and methods for inhibiting the ras-mediated oncogenic and/or transformation process in mammalian cells or tissues.

Growing community of inventors

Tuxedo Park, NY, United States of America

Joseph J Hlavka