Albany Molecular Research, Inc.

Amr Technology, Inc.

Bristol-myers Squibb Compnay

Zhicai Yang

Bruce Francis Molino

David Douglas Manning

Peter C Michels

David John Fairfax

Jun-Ho Maeng

Andreas Peter Termin

Peter D J Grootenhuis

Valentina Molteni

Mark J Suto

Dean Wilson

Long Mao

Angelo J Castellino

Cheng Guo

Michael S Hemenway

Joseph O Rich

Yuri Khmelnitsky

Grant J Carr

Anthony Pechulis

Matthew W Chase

Simon N Haydar

The present invention relates to novel therapeutics with antibacterial activity, processes for their preparation, and pharmaceutical, veterinary and nutritional compositions containing them as active ingredients. The present invention also relates to uses of the novel therapeutics, for example, as medicants or food additives in the treatment of bacterial infections or to aid body mass gain in a subject.

Antibacterial compounds, methods of making them, and uses thereof

Compounds of formulae I and II: are disclosed as 5-HTinhibitors. Those compounds are useful in treating CINV, IBS-D and other diseases and conditions.

2-alkylbenzoxazole carboxamides as 5HT3 modulators

Compounds of formulae I, II and III: are disclosed as 5-HT3 inhibitors. The compounds are useful in treating CINV, IBS-D and other diseases and conditions.

2-aminobenzoxazole carboxamides as 5HT3 modulators

The present invention relates to a process for preparation of a trans ISA247 compound of the formula: where R&#x2550;H or D; R&#x2550;H or D; and R&#x2550;H or D, by application of organozirconium chemistry. The process involves reacting an acetyl cyclosporin aldehyde with an organozirconium reagent to provide acetyl cyclosporin diene (the acetate of trans ISA247) and deacetylating the acetyl cyclosporin diene to produce the trans-isomer of ISA247. The present invention also relates to a process for preparing the same trans ISA247 compound, using olefin cross metathesis. The process involves: olefin cross metathesis of acetyl cyclosporin A to afford acetyl cyclosporin &#x3b1;,&#x3b2;-unsaturated aldehyde; Wittig reaction of the acetyl cyclosporin &#x3b1;,&#x3b2;-unsaturated aldehyde to provide acetyl cyclosporin diene; and deacetylation of the acetyl cyclosporin diene to produce the trans ISA247 compound. Also disclosed are processes for preparing an acetyl cyclosporin &#x3b1;,&#x3b2;-unsaturated aldehyde compound and a cyclosporin triene analogue compound. 

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Compounds of formulae I and II: are disclosed as 5-HTinhibitors. Those compounds that exhibit central activity are useful in treating CINV; those that inhibit peripheral receptors are useful to treat IBS-D.

Benzoxazole carboxamides for treating CINV and IBS-D

The compounds of the present invention are represented by the chemical structure found in Formula I: or a pharmaceutically acceptable salt thereof,

Cyclosporin alkynes and their utility as pharmaceutical agents

The compounds of the present invention are represented by the chemical structure found in Formula I: where A is an amino acid of Formula II: or a pharmaceutically acceptable salt thereof, with R, R, B, C, D, E, F, G, H, I, J, and K defined herein.

Cyclosporins

The compounds of the present invention are represented by Formula I, as shown below: or a pharmaceutically acceptable salt thereof,with X, R, R, and Rdefined herein.

Cyclosporin analogues and their pharmaceutical uses

The compounds of the present invention are represented by the chemical structure found in Formula I: or a pharmaceutically acceptable salt thereof, with X, R, R, and Rdefined herein.

Cyclosporin alkyne analogues and their pharmaceutical uses

The compounds of the present invention are represented by the chemical structure found in Formula I: or a pharmaceutically acceptable salt thereof,with X, R, and Rdefined herein.

Provided herein are novel heteroaromatic substituted cyclopropanes of the Formula (I):as well as compositions, including pharmaceutical compositions, containing the same, and the use thereof in the treatment of various neurological and psychological disorders, e.g., anxiety and depression, treatable by antagonizing CRF receptors.

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Schenectady, NY, United States of America

Zhicai Yang