Topotarget UK Limited

Jsc Grindeks

Oxford Drug Design Limited

Uniwersytet Jagiellonski

Grindeks, a Joint Stock Company

Einars Loza

Ivars Kalvinsh

Paul W Finn

Vija Gailite

Clare J Watkins

Daina Lolya

Igor Starchenkov

James Ritchie

Victor Andrianov

Klara Dikovska

C John Harris

James E S Duffy

Maria Rosario Romero-Martin

Ivars Kalvins

Maija Dambrova

Rasma M Bokaldere

Osvalds Pugovics

Janis Kuka

Kathryn G Moore

Irina Piskunova

Edgars Liepins

Valentina Semenikhina

Reinis Vilskersts

Aigars Jirgensons

Paul William Finn

Aleksandrs Gutcaits

Stefan Chlopicki

Solveiga Grinberga

Maxim Vorona

Ilmars Stonans

Michael Charlton

Olga Habarova

Andris Amolins

Daina Lola

Maria-Rosario Romero-Martin

Grace Edmund

Lluis Ribas De Pouplana

Adelaide Saint-Léger

Viktors Andrianovs

Marina Makrecka

Daina Gustina

Irena Olutnika

Ludmila Serpionova

James E Duffy

James Es Duffy

Adelaide Saint-Leger

Kamil Kus

Victor Adrianov

The present invention pertains generally to the field of therapeutic compounds. More specifically the present invention pertains to certain 2-amino-N-(arylsulfinyl)-acetamide compounds that, inter alia, inhibit (e.g., selectively inhibit) bacterial aminoacyl-tRNA synthetase (aaRS) (e.g., bacterial leucyl-t RNA synthetase, LeuRS). 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 (e.g., selectively inhibit) bacterial aminoacyl-tRNA synthetase; to treat disorders that are ameliorated by the inhibition (e.g., selective inhibition) of bacterial aminoacyl-tRNA synthetase; to treat bacterial infections; etc.

2-amino-N-(arylsulfinyl)-acetamide compounds as inhibitors of bacterial aminoacyl-tRNA synthetase

The present invention relates to novel N-acyl-diarysulfonamides acting as inhibitors of bacterial aminoacyl-tRNA synthetase. These can be used as medicines or as constituent of medicines for the treatment of bacterial infections. 

N-acyl-arylsulfonamide derivatives as aminoacyl-tRNA synthetase inhibitors

Salts of 3-carboxy-N-ethyl-N,N-dimethylpropan-1-aminium, method of preparation thereof and use in the treatment of cardiovascular disease.

Use of 3-carboxy-N-ethyl-N,N-dimethylpropan-1-aminium salts in the treatment of cardiovascular disease

New compound 4-[ethyl(dimethyl)ammonio]butanoate, method of preparation thereof and use in the treatment of cardiovascular disease.

Use of 4-[ethyl(dimethyl)ammonio]butanoate in the treatment of cardiovascular disease

4-[(Haloalkyl)(dimethyl)ammonio]butanoates of formula 

4-[(haloalkyl)(dimethyl)ammonio]butanoates and use thereof in the treatment of cardiovascular disease

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 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 carbamic acid compounds of the formula (I), which inhibit HDAC (histone deacetylase) activity: wherein: J is a linking functional group and is independently:&#x2014;O &#x2014;C(&#x2550;O)&#x2014; or &#x2014;C(&#x2550;O)&#x2014;O &#x2014; or &#x2014;C(&#x2550;O)&#x2014;; Cy is a cyclyl group and is independently: Ccarbocyclyl, Cheterocyclyl, or Caryl; and is optionally substituted; Qis a cyclyl leader group, and is independently a divalent bidentate group obtained by removing two hydrogen atoms from a ring carbon atom of a saturated monocyclic hydrocarbon having fromtoring atoms, or by removing two hydrogen atoms from a ring carbon atom of saturated monocyclic heterocyclic compound having fromtoring atoms includingnitrogen ring atom oroxygen ring atom; and is optionally substituted; Qis an acid leader group, and is independently: Calkylene; and is optionally substituted; or: Qis an acid leader group, and is independently: Carylene; Carylene-Calkylene; Calkylene-Carylene; or Calkylene-CaryleneCalkylene; and is optionally substituted; 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 an ester or ketone linkage as HDAC inhibitors

This invention pertains to certain active carbamic acid compounds which inhibit HDAC activity and which have the following formula: (1) 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.

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Riga, Latvia

Einars Loza