Glaxo Group Limited

Convergence Pharmaceuticals Limited

Simon Edward Ward

Kevin Thewlis

Paul John Beswick

Daniele Andreotti

David Norton

Colin Philip Leslie

Barbara Bertani

Markus Bergauer

Robert James Gleave

Sadie Vile

Stephen Harrison

Jessica Tibasco

Simone Spada

Domenica Antonia Pizzi

Alessandro Falchi

Daniel Marcus Bradley

Matteo Biagetti

Giancarlo Merlo

Marilisa Rinaldi

Luigi Piero Stasi

Antonio Kuok Keong Vong

Shuji Hachisu

Steven Mark Bromidge

Wai Ngor Chan

Jag Paul Heer

Roberto Profeta

Paul William Smith

Luca Arista

Francesca Cardullo

Frank P Harrington

Helen Susanne Price

Nicolas Bertheleme

Jaqueline Sandra Scott

Nicholas Bertheleme

Kevin Michael Thewlis

The present invention relates to novel tetrazole compounds; to processes for their preparation; to pharmaceutical compositions containing the compounds; and to the use of the compounds in therapy to treat diseases for which blocking the Ca2.2 calcium channels is beneficial. Formula (I) wherein A is: (II) or (III)  

Tetrazole compounds as calcium channel blockers

The present invention relates to novel tetrazole compounds of Formula (I) wherein A is (II) or (III); to processes for their preparation; to pharmaceutical compositions containing the compounds; and to the use of the compounds in therapy to treat diseases for which blocking the Ca2.2 calcium channels is beneficial. wherein A is 

The invention relates to novel piperazine compounds of formula (I): to processes for their preparation; to pharmaceutical compositions containing the compounds; and to the use of the compounds in therapy to treat diseases for which blocking the Cav2.2 calcium channels is beneficial, i.e. in particular to treat pain.

Tricyclic substituted benzenesulfonamide piperazine derivatives as CAV2.2 calcium channel blockers

Compounds of formula (I) and salts thereof are provided: wherein n is 0, 1, 2 or 3; Ris selected from phenyl and pyridyl, each of which is optionally substituted by one or two groups independently selected from Calkyl and halogen; and Ris selected from H and CHwhen n is 1 and Ris H when n is 2 or 3. Processes for preparation, pharmaceutical compositions, and uses thereof as a medicament, for example in the treatment of a disease or condition mediated by a reduction or imbalance in glutamate receptor function, such as schizophrenia or cognition impairment, are also disclosed. 

Compounds which potentiate the AMPA receptor and uses thereof in medicine

The present invention relates to novel piperazine derivatives; to processes for their preparation; to pharmaceutical compositions containing the derivatives; and to the use of the derivatives in therapy to treat diseases for which blocking the Ca2.2 calcium channels is beneficial.

Pyrazolo[1,5-A]pyrimidine-carbonyl-piperazine derivatives

This invention relates to potentiation of the glutamate receptor by novel compounds of formula (I):  The invention also relates to the use of the derivatives in treating diseases and conditions mediated by potentiation of the glutamate receptor, compositions containing the derivatives and processes for their preparation.

Compounds which potentiate glutamate receptor and uses thereof in medicine

This case discloses compounds of formula (I) wherein Ris Calkyl, haloCalkyl, Calkenyl, amino, monoCalkylamino or diCalkylamino; Rand R, which may be the same or different, are hydrogen, halogen, Calkyl, haloCalkyl, Calkoxy, haloCalkoxy, cyano or amino; each R, which may be the same or different, is Calkyl, halogen, haloCalkyl, Calkoxy, haloCalkoxy, cyano, nitro or amino; p is 0, 1 or 2; each R, which may be the same or different, is Calkyl, halogen, haloCalkyl, Calkoxy, haloCalkoxy, cyano, nitro or amino; q is 0, 1 or 2; Ris &#x2014;NRSOR, &#x2014;NRC(&#x2550;O)R, &#x2014;NR(C&#x2550;O)N(R), &#x2014;(C&#x2550;O)R, &#x2014;CHNRSOR, &#x2014;CHNRC(&#x2550;O)R, CHNR(C&#x2550;O)N(R)or &#x2014;CH(C&#x2550;O)R; where Rand each R, which may be the same or different, is hydrogen or Calkyl; Rand Rare Calkyl or haloCalkyl; or Rand R, or Rand R, together with the interconnecting atoms, may form a 5- or 6-membered ring; n is 1 or 2; and Rand R, which may be the same or different, are hydrogen, halogen, Calkyl, haloCalkyl, Calkoxy, haloCalkoxy, cyano or amino. It also discloses methods for preparing the compounds and their use in therapy such as treating schizophrenia. 

Disclosed are methods for the preparation of compounds of formula (I): wherein R, m, X, R, n, W, p, Y, Z, R, R, Rand q have the meanings as defined in the description.

Quinoline and quinazoline derivatives having affinity for 5HT1-type receptors

Compounds of formula (I) and salts are provided: along with pharmaceutical compositions, uses in treating a disease or condition mediated by a reduction or imbalance in glutamate receptor function such as schizophrenia or cognition impairment.

Compounds which potentiate AMPA receptor and uses thereof in medicine

Compounds of formula (I) or a pharmaceutically acceptable salt, solvate or prodrug thereof, are disclosed: wherein Ris Calkyl, haloCalkyl, Calkenyl, amino, monoCalkylamino or diCalkylamino; Rand R, which may be the same or different, are hydrogen, halogen, Calkyl, haloCalkyl, Calkoxy, haloCalkoxy, cyano, amino, monoCalkylamino or diCalkylamino; each R, which may be the same or different, is Calkyl, halogen, Calkyl, haloCalkyl, Calkoxy, haloCalkoxy, cyano, nitro, amino, monoCalkylamino or diCalkylamino; p is 0, 1 or 2; n is 1 or 2; Rand R, which may be the same or different, are hydrogen, halogen, Calkyl, haloCalkyl, Calkoxy, haloCalkoxy, cyano, amino, monoCalkylamino or diCalkylamino; and Het is thienyl, pyridyl, pyrimidinyl, pyridazinyl, pyrimidinyl, pyrazinyl, imidazolyl, pyrazolyl, pyrrolyl, quinolyl, thiazolyl or furyl, each of which may be substituted by one or more groups independently selected from the list consisting of Calkyl, Calkoxy, acetyl, halogen, haloCalkyl, cyano, nitro, amino, monoCalkylamino and diCalkylamino. Methods of preparation of the compounds, and uses thereof in medicine, for example treatment of schizophrenia, are also disclosed.

Disclosed are methods for use of compounds of formula (I) in combination with other active substances in the treatment of CNS disorders such as depression or anxiety. wherein R, m, X, R, n, W, p, Y, Z, R, R, Rand q have the meanings as defined in the description.

Compounds of formula (I) and salts are provided: along with pharmaceutical compositions, uses in medicine, e.g., treating disease or condition mediated by a reduction or imbalance in glutamate receptor function, such as schizophrenia or cognition impairment.

Compounds of formula (I) and pharmaceutically acceptable salts thereof are disclosed: wherein A is optionally substituted phenyl, naphthyl, indolyl, quinolinyl, quinazolinyl, indazolyl, isoquinolinyl or benzofuranyl; b is 1, 2 or 3 and c is 1, 2 or 3, wherein b+c is 2, 3, 4 or 5; X is carbon, Y is CH, is a double bond and e is 0; or X is carbon, Y is CHor oxygen, is a single bond and e is 1; or X is nitrogen, Y is CH, is a single bond and e is 0; R1 is hydrogen, cyano, halogen, Calkyl, Calkoxy, CalkoxyCalkyl, NHCOCHor OCONR5R6, wherein R5 and R6 are independently hydrogen or Calkyl; R2 is halogen, cyano or Calkoxy; d is 0, 1, 2 or 3; R3 is hydrogen, Calkyl, Calkanoyl, fluoroCalkanoyl, Calkylsulfonyl, fluoroCalkylsulfonyl, carbamoyl, Calkylcarbamoyl or arylCalkyl; and R4, together with the nitrogen atom to which it is attached, forms an optionally substituted 5 to 7 membered heterocyclic group fused to the benzene ring, provided that when a compound of formula (I) has the following structure: wherein A, b, c, R1, e, X, Y, R2 and d are as defined above and R3 is hydrogen, Calkyl or arylCalkyl, then (i) X is carbon, Y is CH and is a double bond; or (ii) b and c are both 1; or (iii) the carbon atom adjacent to the oxo-substituted carbon atom in the morpholinyl ring, marked '&#x2605;', is substituted. Methods of preparing the compounds and uses of the compounds in therapy, in particular for a CNS disorder such as depression or anxiety, are also disclosed.

[object Object]

Compounds of formula (I) and pharmaceutically acceptable salts thereof are disclosed: wherein: A is optionally substituted phenyl, naphthyl, indolyl, quinolinyl, quinazolinyl, indazolyl, isoquinolinyl or benzofuranyl; X is carbon, Y is CH and is a double bond; or X is CH, Y is CHor oxygen and is a single bond; or X is nitrogen, Y is CHand is a single bond; R 1 is halogen, cyano, or Calkoxy; a is 0,1, 2 or 3 ; b is 0 or 1 ; R 2 is hydrogen, Calkyl, Calkanoyl, fluoroCalkanoyl, Calkylsulfonyl, fluoroCalkylsulfonyl, carbamoyl, Calkylcarbamoyl or arylCalkyl; and R 3 , together with the nitrogen atom to which it is attached, forms an optionally substituted 5 to 7 membered heterocyclic group fused to the benzene ring. Methods of preparing the compounds and uses of the compounds in therapy, in particular for a CNS disorder such as depression or anxiety, are also disclosed.

Growing community of inventors

Harlow, United Kingdom

Simon Edward Ward