Topotarget UK Limited

Clare J Watkins

Ivars Kalvinsh

Einars Loza

Paul W Finn

Igor Starchenkov

James Ritchie

Vija Gailite

Klara Dikovska

Daina Lolya

James E S Duffy

C John Harris

Maria Rosario Romero-Martin

Victor Andrianov

Maxim Vorona

Kathryn G Moore

Rasma M Bokaldere

Valentina Semenikhina

Irina Piskunova

Maria-Rosario Romero-Martin

Andris Amolins

James E Duffy

James Es Duffy

This invention pertains to certain carbamic acid compounds which inhibit HDAC (histone deacetylase) activity of the following formula: 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 in the treatment of conditions mediated by HDAC, cancer, proliferative conditions, psoriasis, etc.

Carbamic acid compounds comprising a piperazine 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; 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 carbamic acid compounds which inhibit HDAC (histone deacetylase) activity of the following formula: wherein: Cy is independently a cyclyl group; Qis independently a covalent bond or cyclyl leader group; the piperazin-1,4-diyl group is optionally substituted; Jis independently a covalent bond or &#x2014;C(&#x2550;; O)&#x2014;; Jis independently &#x2014;C(&#x2550;O)&#x2014; or &#x2014;S(&#x2550;O)&#x2014;; Qis independently an acid leader group; wherein: Cy is independently: Ccarbocyclyl, Cheterocyclyl, or Caryl; and is optionally substituted; Qis independently: a covalent bond; Calkylene; or Calkylene-X&#x2014;Calkylene, &#x2014;X&#x2014;Calkylene, or Calkylene-X&#x2014;, wherein X is &#x2014;O&#x2014; or &#x2014;S&#x2014;; and is optionally substituted; Qis independently: Calkylene; and is optionally substituted; and has a backbone length of at least 4 atoms; or: Qis independently: Carylene; Carylene-Calkylene; Calkylene-Carylene; or, Calkylene-Carylene-Calkylene; and is optionally substituted; and has a backbone length of at least 4 atoms; or a pharmaceutically acceptable salt, solvate, amide, ester, ether, chemically protected form, or prodrug 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 in the treatment of conditions mediated by HDAC, cancer, proliferative conditions, psoriasis, etc.

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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Abingdon, United Kingdom

Clare J Watkins