Topotarget UK Limited

Merz Pharma Gmbh & Co Kgaa

Merz+co. Gmbh & Co.

Taiho Pharmaceutical Company Limited

Valsts Zinatniska Iestade - Bezpelnas Organizacija Latvijas Organiskas

Ivars Kalvinsh

Einars Loza

Wojciech Danysz

Valerjans Kauss

Paul W Finn

Vija Gailite

Aigars Jirgensons

Markus Henrich

Markus R Gold

Clare J Watkins

Igor Starchenkov

Daina Lolya

James Ritchie

Victor Andrianov

Christopher Graham Raphael Parsons

Klara Dikovska

James E S Duffy

C John Harris

Maria Rosario Romero-Martin

Tanja Weil

Maksims Vanejevs

Kathryn G Moore

Rasma M Bokaldere

Maxim Vorona

Irina Piskunova

Aleksandrs Gutcaits

Claudia Jatzke

Christopher Graham Parsons

Valentina Semenikhina

Jens Nagel

Andrzej Dekundy

Ieva Jaunzeme

Mirko Hechenberger

Juris Fotins

Ronalds Zemribo

Maria-Rosario Romero-Martin

Olga Habarova

Andris Amolins

Yasushi Abiko

Irena Olutnika

Ludmila Serpionova

Christopher G R Parsons

John M Kelly

Eugene Rozhkov

Irene Piskunova

Kiyotaka Tajima

Maris Veveris

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

Substituted pyrazolopyrimidine derivatives of formula (I) wherein

Substituted pyrazolo[1,5-A]pyrimidines as metabotropic glutamate receptor modulators

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

The invention relates to pyrazolopyrimidine derivatives of formula (I) wherein

Substituted pyrazolo[1,5-a]pyrimidines as metabotropic glutamate receptor modulators

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.

The invention relates to tetrahydroquinolinone derivatives as well as their pharmaceutically acceptable salts. The invention further relates to a process for the preparation of such compounds. The compounds of the invention are group I mGluR antagonists and are therefore useful for the control and prevention of acute and/or chronic neurological disorders.

Tetrahydroquinolinones and their use as antagonists of metabotropic glutamate receptors

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

The invention relates to ethynyl-substituted tetrahydroquinolinone derivatives as well as their pharmaceutically acceptable salts. The invention further relates to a process for the preparation of such compounds. The compounds of the invention are group I mGluR modulators and are therefore useful for the control and prevention of acute and/or chronic neurological disorders.

Tetrahydroquinolones and their use as modulators of metabotropic glutamate receptors

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.

Azabicyclic, azatricyclic and azaspirocyclic derivatives of aminocyclohexanes which are systemically-active as NMDA, 5HT, and nicotinic receptor antagonists, pharmaceutical compositions comprising the same, method of preparation thereof, and method of treating CNS disorders which involve disturbances of glutamatergic, serotoninergic, and nicotinic transmission, treating immunomodulatory disorders, and antimalaria, antitrypanosomal, anti-Borne virus, anti-HSV and anti-Hepatitis C virus activity.

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Riga, Latvia

Ivars Kalvinsh