Bristol-myers Company

Vion Pharmaceuticals, Inc.

Bristol-myers Squibb Compnay

E. R. Squibb Sons, Inc.

Gemin X Pharmaceuticals Canada Inc.

Gemin X Biotechnologies Inc.

Gemin X Pharmaceuticals Canada Inc./gemin X Pharmaceutiques Canada Inc.

Terrence W Doyle

Takushi Kaneko

Dolatrai M Vyas

John M Essery

Henry Schmitz

Yulin Chiang

Bernard R Belleau

Terry T Conway

Richard A Partyka

Henry S Wong

James A Bush

Donald E Nettleton, Jr

William T Bradner

Bing Yu Luh

Elise Rioux

Xu Kevin Lin

Jean-Francois Lavallee

Giorgio Attardo

James A Matson

Shu-Hui Chen

Edward Meyers

Wen-Chih Liu

Ivan C King

Veeraswamy Manne

Xiuyan Li

Robert W Myllymaki

Jun Li

Yang Xu

Yasutsugu Ueda

Samuel C Fortin

Vittorio Farina

Sasmita Tripathy

Amarendra B Mikkilineni

Xavier Billot

John Mao

Michael Belcourt

Qi Qiao

Chuan-Sheng Niu

ChuanSheng Niu

Laurent Belec

Daniel Rabouin

Bing-Yu Luh

Srinivasa Karra

David L Johnson

Zujin Li

Kenza Dairi

Michael F Belcourt

The present invention relates to novel Triheterocyclic Compounds, compositions comprising a Triheterocyclic Compound, and methods useful for treating or preventing cancer or a neoplastic disorder comprising administering a Triheterocyclic Compound. The compounds, compositions, and methods of the invention are also useful for inhibiting the growth of a cancer cell or neoplastic cell, treating or preventing a viral infection, or inhibiting the replication and/or infectivity of a virus.

Methods for treating cancer

Triheterocyclic compounds, compositions, and methods for treating cancer or viral diseases

Novel phosphate-bearing prodrugs of sulfonyl hydrazines have the formula presented below. Pharmaceutical compositions and uses thereof in the treatment of cancer are claimed. The aforementioned prodrugs include enantiomers, stereoisomers and tautomers thereof, as well as pharmaceutically acceptable salts or solvates and metabolites from all stages. The aforementioned prodrugs are preferentially activated in hypoxic tumors and can be given either alone, or in combination with other anticancer agents or with phototheraphy or radiotherapy. where R is C-Calkyl or haloalkyl;

Phosphate-bearing prodrugs of sulfonyl hydrazines as hypoxia-selective antineoplastic agents

The present invention relates to Diterpenoid Compounds, compositions comprising an effective amount of a Diterpenoid Compound, and methods useful for treating or preventing cancer or a neoplastic disorder comprising administering an effective amount of a Diterpenoid Compound. The compounds, compositions, and methods of the invention are also useful for inhibiting the growth of a cancer cell or neoplastic cell, or for inducing apoptosis in a cancer or neoplastic cell. The compounds, compositions, and methods of the invention are further useful for treating or preventing a fungal infection. The compounds, compositions, and methods of the invention are also useful for inhibiting the growth of a fungus.

Diterpenoid compounds, compositions thereof and their use as anti-cancer or anti-fungal agents

The present invention relates to compounds according to the structure (I):Where R is &#x2014;CHor &#x2014;CHCHCl; R' is C-Calkyl or &#x2014;CHCHCl; Ror Ris OPOH, NO, OCO(Glu-OH), NHCO(Glu-OH), NHRand unassigned groups of R, R, R, Rand Rare, independently H, F, Cl, Br, I, OH, OPOH, OCH, CF, OCF, NO, CN, SOCH, SOCF, COCH, COOCH, SCH, SF, NH, NHR, N(CH), OPOH, or a C1-C7 alkyl group with the proviso that when any two of unassigned groups of R, R, R, Ror Rare other than H, the other two of unassigned groups of R, R, R, Ror Rare H. Ris H or polyglutamyl as described. Phosphoric acid and glutamic acid can be a free acid or pharmaceutically acceptable salt thereof.

Water-soluble SHPs as novel alkylating agents

Modified prodrug forms of AP/AMP

The present invention relates to improved, efficient chemical syntheses of 3-aminopyridine-2-carboxaldehyde thiosemicarbazone (3-AP) and 3-amino-4-methylpyridine-2-carboxaldehyde thiosemicarbazone (3-AMP).

Process for the synthesis of ribonucleotide reductase inhibitors 3-AP

The present invention relates to novel prodrug forms of ribonucleoside diphosphate reductase inhibitors 3-aminopyridine-2-carboxaldehyde thiosemicarbazone (3-AP) 3-amino-4-methylpyridine-2-carboxaldehyde thiosemicarbazone (3-AMP) which have increased water solubility, bioavailablity and resistance to in vivo acetylation of their amino functions. Novel compounds according to the present invention relate to those of the formula: ##STR1## where R.sup.4 is H or CH.sub.3 and

Prodrug forms of ribonucleotide reductase inhibitors 3-AP and 3-AMP

This invention relates to a compound of formula I ##STR1## or a pharmaceutically acceptable salt thereof, in which R.sup.2 is a radical of the formula ##STR2## in which R.sup.a and R.sup.b are independently hydrogen or C.sub.1-6 alkyl, said C.sub.1-6 alkyl being optionally substituted with hydroxy, phosphono, phosphonooxy, carboxy or di(C.sub.1-6 alkyl) amino; or NR.sup.a R.sup.b together represents a radical of the formula ##STR3## in which y is one to three, and R.sup.a is as defined above; R.sup.p and R.sup.r are independently same or different C.sub.1-6 alkyl;

Benzoate derivatives of taxol

The present invention provides novel mitomycin analogs containing a cyclic acetal or thioacetal group. These compounds are mitomycin C analogs in which the 7-amino group bears a 5-membered heterocyclic substituent. Mitomycin C is an antitumor agent of established utility, and the 7-N-substituted mitosane analogs thereof have similar utility.

Mitomycin analogs

10'-Desmethoxystreptonigrin, obtainable by cultivation of a strain of Streptomyces albus, A.T.C.C. No. 55161, and salts, esters and amides thereof. The novel compounds have antitumor and antibiotic activity.

10'desmethoxystreptonigrin production by Streptomyces albus

The present invention is directed to novel taxol derivatives useful as anti-tumor agents. Also provided by this invention is pharmaceutical formulations and methods of treating mammalian tumors with the compounds of this invention.

Phosphonooxy and carbonate derivatives of taxol

10'-Desmethoxystreptonigrin

The present invention provides novel mitomycin analogs containing a disulfide group and processes for the preparation thereof. These compounds are mitomycin A analogs in which the 7-alkoxy group bears an organic substituent incorporating a disulfide group. Mitomycin A is an antibiotic of established utility, and the 7-O-substituted mitosane analogs thereof have similar utility.

Substituted 7-oxomitosanes

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Fayetteville, NY, United States of America

Terrence W Doyle