Topotarget UK Limited

Action Pharma A/s

Acure Pharma Ab

Victor Andrianov

Ivars Kalvinsh

Einars Loza

Paul W Finn

James Ritchie

Vija Gailite

Daina Lolya

Clare J Watkins

Igor Starchenkov

Klara Dikovska

James E S Duffy

C John Harris

Maria Rosario Romero-Martin

Kathryn G Moore

Maxim Vorona

Irina Piskunova

Anna Skottner

Torbjörn Lundstedt

Arne Boman

Per Andersson

Elisabeth Seifert

Rasma M Bokaldere

Valentina Semenikhina

Maria-Rosario Romero-Martin

Andris Amolins

Olga Habarova

Ivars Kalvins

James E Duffy

James Es Duffy

This invention pertains to certain carbamic acid compounds of the following formula, which inhibit HDAC (histone deacetylase) activity wherein: A is independently an unsubstituted or substituted bicyclic Cheteroaryl group (e.g., quinolinyl; quinoxalinyl; benzoxazolyl; benzothiazolyl); Q is an acid leader group, and is independently an unsubstituted or substituted, saturated or unsaturated Calkylene group having a backbone length of 4 or less; with the proviso that if A is unsubstituted benzothiazol-2-yl, then Q is an unsaturated group; and with the proviso that if A is unsubstituted quinolin-6-yl, then Q is unsubstituted at the &#x3b1;-position; and with the proviso that A is not benzimidazol-2-yl; 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 in the treatment of conditions mediated by HDAC, cancer, proliferative conditions, psoriasis, etc.

Carbamic acid compounds comprising a bicyclic heteroaryl group 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 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.

The present invention provides novel compounds of the general Formula (I) as ligands to the melanocortin receptors and/or for treatment of disorders in the melanocortin system:  

N-phenylpyrrole guanidine derivatives as melanocortin receptor ligands

The present invention provides novel compounds of the general Formula (I) as ligands to the melanocortin receptors and/or for treatment of disorders in the melanocortin system: wherein X is (CH)where n is 0, 1 or 2; 

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

The present invention provides novel compounds and use of compounds of general formula (I) as ligands to the melanocortin receptors and/or for treatment of disorders in the melanocortin system: Wherein X and Y are independently chosen from O, N, S and (CH), where n is 0, 1, 2, 3, 4, or 5, or a combination of these and may contain carbon-carbon multiple bonds and branched chains as well as alicyclic and heterocyclic groups; Q is H or OH; Rand Rcan be either the same or different and are chosen from hydrogen or the residue of an aromatic group as listed in Scheme 1 and the pharmacologically active salts thereof 

Compounds acting as melanocortin receptor ligands

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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Riga, Latvia

Victor Andrianov