Topotarget UK Limited

James E S Duffy

Ivars Kalvinsh

Einars Loza

Paul W Finn

Clare J Watkins

Igor Starchenkov

Maria Rosario Romero-Martin

C John Harris

James Ritchie

Victor Andrianov

Vija Gailite

Klara Dikovska

Kathryn G Moore

Maxim Vorona

Daina Lolya

Rasma M Bokaldere

Valentina Semenikhina

Irina Piskunova

Andris Amolins

This invention pertains to certain active carbamic acid compounds which inhibit HDAC activity and which have the formula (1) wherein: A is an aryl group; Qis an aryl leader group having a backbone of at least 2 carbon atoms; J is an amide linkage selected from: &#x2014;NRC(&#x2550;O)&#x2014; and &#x2014;C(&#x2550;O)NR&#x2014;; Ris an amido substituent; and, Qis an acid leader group; and pharmaceutically acceptable salts, solvates, amides, esters, ethers, chemically protected forms, and prodrugs thereof. The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo, to inhibit HDAC, and, e.g., to inhibit proliferative conditions, such as cancer and psorias.

Carbamic acid compounds comprising an amide linkage as HDAC inhibitors

This invention pertains to certain active carbamic acid compounds which inhibit HDAC activity and which have the formula (1) wherein: A is an aryl group; Q1 is an aryl leader group having a backbone of at least 2 carbon atoms; J is an amide linkage selected from: &#x2014;NR1C(&#x2550;O)&#x2014; and &#x2014;C(&#x2550;O)NR1-; R1 is an amido substituent; and, Q2 is an acid leader group; and pharmaceutically acceptable salts, solvates, amides, esters, ethers, chemically protected forms, and prodrugs thereof. The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo, to inhibit HDAC, and, e.g., to inhibit proliferative conditions, such as cancer and psoriasis.

This invention pertains to certain active carbamic acid compounds which inhibit HDAC activity and which have the following formula: (I) A is an aryl group; Qis a covalent bond or an aryl leader group; J is a sulfonamide linkage selected from: &#x2014;S(&#x2550;O)NR&#x2014; and &#x2014;NRS(&#x2550;O)&#x2014;; Ris a sulfonamido substituent; and, Qis an acid leader group; with the proviso that if J is &#x2014;S(&#x2550;O)NR&#x2014;, then Qis an aryl leader group; and pharmaceutically acceptable salts, solvates, amides, esters, ethers, chemically protected forms, and prodrugs thereof. The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo, to inhibit HDAC, and, e.g., to inhibit proliferative conditions, such as cancer and psoriasis.

Carbamic acid compounds comprising a sulfonamide linkage as HDAC inhibitors

This invention pertains to certain active carbamic acid compounds which inhibit HDAC activity and which have the following formula:wherein: A is an aryl group; Qis a covalent bond or an aryl leader group; J is an amide linkage selected from: &#x2014;NRC(&#x2550;O)&#x2014; and &#x2014;C(&#x2550;O)NR&#x2014;; Ris an amido substituent; X is an ether heteroatom, and is &#x2014;O&#x2014; or &#x2014;S&#x2014;; and, Rand Rare each independently an ether group; and pharmaceutically acceptable salts, solvates, amides, esters, ethers, chemically protected forms, and prodrugs thereof. The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo, to inhibit HDAC, and, e.g., to inhibit proliferative conditions, such as cancer and psoriasis.

Carbamic acid compounds comprising an ether linkage as HDAC inhibitors

This invention pertains to certain active carbamic acid compounds which inhibit HDAC activity and which have the following formula: (I) A is an aryl group; Qis a covalent bond or an aryl leader group; J is a sulfonamide linkage selected from: &#x2014;S(&#x2550;O)NR&#x2014; and &#x2014;NRS(&#x2550;O)&#x2014;; R1 is a sulfonamido substituent; and, Qis an acid leader group; with the proviso that if J is &#x2014;S(&#x2550;O)NR&#x2014;, then Qis an aryl leader group; and pharmaceutically acceptable salts, solvates, amides, esters, ethers, chemically protected forms, and prodrugs thereof. The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo, to inhibit HDAC, and, e.g., to inhibit proliferative conditions, such as cancer and psoriasis.

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Sittingbourne, United Kingdom

James E S Duffy