Ctxt Pty Limited

Cancer Therapeutics Crc Pty Limited

Scott Raymond Walker

Richard Charles Foitzik

Michelle Ang Camerino

Paul Anthony Stupple

Ylva Elisabet Bergman

Danny Ganame

Ian Peter Holmes

Romina Lessene

Catherine Fae Hemley

Gillian Elizabeth Lunniss

H Rachel Lagiakos

Benjamin Joseph Morrow

Neil Choi

Marica Nikac

Ylva Elisabet Bergman Bozikis

Wilhelmus Johannes Antonius Kersten

John Feutrill

Alexandra Elizabeth Stupple

Helen Rachel Lagiakos

Graeme Irvine Stevenson

Yiva Bergman

Ylva Bergman

Jonathan Grant Hubert

Marcia Nikac

Neil Chol

George Nikolakopoulos

Gillian Elizabeth Lunnis

Jo-Anne Pinson

A compound of formula (I), or a pharmaceutical salt thereof:

Compounds

A compound of formula (I), or a pharmaceutically acceptable salt thereof.

A compound of formula (I), wherein Ris selected from (i) H, (ii) Ccycloalkyl, (iii) Cheterocyclyl optionally substituted with a group selected from: methyl and ester, and (iv) linear or branched Calkyl optionally substituted with a group selected from: alkoxy, amino, amido, acylamido, acyloxy, alkyl carboxyl ester, alkyl carbamoyl, alkyl carbamoyl ester, phenyl, phosphonate ester, Cheterocyclyl optionally substituted with a group selected from methyl and oxo, and a naturally occurring amino acid, optionally N-substituted with a group selected from methyl, acetyl and boc; Ais CRor N; Ais CRor N; Ais CRor N; Ais CRor N; where no more than two of A, A, A, and Amay be N; one or two of R, R, R, and R, (if present) are selected from H, F, Cl, Br, Me, CF, cyclopropyl, cyano, OMe, OEt, CHOH, CHOMe and CHNMe; the remainder of R, R, R, and R, (if present) are H; Y is O, NH or CH; Ris selected from: (RYA) and (RYB).

Substituted condensed thiophenes as modulators of sting

A compound of formula (Ia), (Ib) or (Ic) wherein: n is 1 or 2; Ris H or Me; Ris optionally one or more halo or methyl groups; Rand Rare independently selected from the group consisting of: (i) F; (ii) H; (iii) Me; and (iv) CHOH; Rand R(if present) are independently selected from the group consisting of: (i) F; (ii) H; (iii) Me; and (iv) CHOH; Rand Rare independently selected from H and Me; Ris selected from OH, &#x2014;NH, &#x2014;C(&#x2550;O)NH, and &#x2014;CHOH; Ris either H or Me; X is either N or CH; Ris selected from H and Calkyl; (a) one of R, R, Rand Ris selected from H, halo, Calkyl, Calkoxy, NHCalkyl; (b) another of R, R, Rand Ris selected from H, Calkyl, Cfluoroalkyl, Ccycloalkyl, Cheteroaryl, Cheteroaryl methyl, Cheterocyclyl, Cheterocyclyl methyl, phenyl, benzyl, halo, amido, amidomethyl, acylamido, acylamidomethyl, Calkyl ester, Calkyl ester methyl, Calkyl carbamoyl, Calkyl carbamoyl methyl, Calkylacyl, Calkylacyl methyl, phenylcarbonyl, carboxy, carboxymethyl, ether, amino, amino methyl, sulfonamido, sulfonamino, sulfone, sulfoxide, nitrile and nitrilemethyl; (c) the others of R, R, Rand Rare H. 

PRMT5 inhibitors

A compound of formula (I) wherein: Ris optionally one or more halo or methyl groups; Rand Rare independently selected from the group consisting of: (i) F; (ii) H; (iii) Me; and (iv) CHOH; Rand Rare independently selected from the group consisting of: (i) F; (ii) H; (iii) Me; and (iv) CHOH; Rand Rare independently selected from H and Me; Ris either H or Me; Ris either H or Me; A is either (i) optionally substituted phenyl; (ii) optionally substituted naphthyl; or (iii) optionally substituted Cheteroaryl. 

Tetrahydroisoquinoline derived PRMT5-inhibitors

A compound of formula (I) wherein: n is 1 or 2; p is 0 or 1; R, R, Rand Rare independently selected from H, halo, methyl and methoxy; Rand Rare independently selected from the group consisting of: (i) F; (ii) H; (iii) Me; and (iv) CHOH; Rand Rare independently selected from the group consisting of: (i) F; (ii) H; (iii) Me; and (iv) CHOH; Ris H or Me; Rand Rare independently selected from H and Me; Ris either H or Me; Rand Rare independently selected from H and Me; X is either N or CH; Ris selected from H and Calkyl; (a) one of R, R, R, and Ris selected from H, halo, Calkyl, Calkoxy, NHCalkyl; (b) another of R, R, Rand Ris selected from H, Calkyl, Cfluoroalkyl, Ccycloalkyl, Cheteroaryl, Cheteroaryl methyl, Cheterocyclyl, Cheterocyclyl methyl, phenyl, benzyl, halo, amido, amidomethyl, acylamido, acylamidomethyl, Calkyl ester, Calkyl ester methyl, Calkyl carbamoyl, Calkyl carbamoyl methyl, Calkylacyl, Calkylacyl methyl, phenylcarbonyl, carboxy, carboxymethyl, ether, amino, amino methyl, sulfonamido, sulfonamino, sulfone, sulfoxide, nitrile and nitrilemethyl; (c) the others of R, R, Rand Rare H. 

Tetrahydroisoquinolines as PRMT5 inhibitors

A compound of formula I wherein: n is 1 or 2: p is 0 or 1; Ris optionally one or more halo or methyl groups; Rand Rare independently selected from the group consisting of: (i) F; (ii) H; (iii) Me; and (iv) CHOH; Rand Rare independently selected from the group consisting of: (i) F; (ii) H; (iii) Me; and (iv) CHOH; Rand Rare independently selected from H and Me; Ris either H or Me; Ris either H or Me; Rand Rare independently selected from H and Me; A is either (i) optionally substituted phenyl; (ii) optionally substituted naphthyl; or (iii) optionally substituted Cheteroaryl. 

A compound of formula (I) wherein: n is 1 or 2; p is 0 or 1; R, R, Rand Rare independently selected from the group consisting of H, halo, Calkoxy, Calkyl, Cfluoroalkyl, Ccycloalkyl, NH&#x2014;Calkyl and cyano; Rand Rare independently selected from the group consisting of: (i) F; (ii) H; (iii) Me; and (iv) CHOH; Rand Rare independently selected from the group consisting of: (i) F; (ii) H; (iii) Me; and (iv) CHOH; Ris H or Me; Rand Rare independently selected from H and Me; Ris either H or Me; Ris either H or Me; Rand Rare independently selected from H and Me; A is either (i) optionally substituted phenyl; (ii) optionally substituted naphthyl; or (iii) optionally substituted Cheteroaryl; wherein when Ris H, at least one of R, R, Rand Ris selected from Calkoxy, Calkyl, Cfluoroalkyl, Ccycloalkyl, NH&#x2014;Calkyl and cyano. 

A compound of formula (1a), (1b) or (1c) wherein: n is 1 or 2; Ris H or Me; Ris optionally one or more halo or methyl groups; Rand Rare independently selected from the group consisting of: (i) F; (ii) H; (iii) Me; and (iv) CHOH; Rand R(if present) are independently selected from the group consisting of: (i) F; (ii) H; (iii) Me; and (iv) CHOH; Rand Rare independently selected from H and Me; Ris selected from OH, &#x2014;NH, &#x2014;C(&#x2550;O)NH, and &#x2014;CHOH; Ris either H or Me; Ris either H or Me; A is either (i) optionally substituted phenyl; (ii) optionally substituted naphthyl; or (iii) optionally substituted Cheteroaryl. 

Aminoindane-, aminotetrahydronaphthalene- and aminobenzocyclobutane-derived PRMT5-inhibitors

Substituted benzimidazole and 3H-imidazo[4,5-b]pyridines or formula I: where X and Y respectively are selected from: (i) N and N; and (ii) N and CR; Ais selected from: a Cheteroarylene group, containing 2 or 3 ring heteroatoms, where the bonds to L1 and the core are &#x3b2; to one another; Lis selected from: (i)&#x2014;O&#x2014;CH&#x2014;; (ii)&#x2014;CH&#x2014;O&#x2014;; (iii)&#x2014;C(&#x2550;O)&#x2014;NH&#x2014;; (iv)&#x2014;CH(OH)&#x2014;; (v)&#x2014;CH&#x2014;NH&#x2014;C(&#x2550;O)&#x2014;; (vi)&#x2014;S&#x2014;CH&#x2014;; (vii)&#x2014;CH&#x2014;S&#x2014;; (viii)&#x2014;CH&#x2014;; and (ix)&#x2014;CH(CH)&#x2014;O&#x2014;; A1 is phenyl, optionally substituted by F or CF; their use as pharmaceuticals, and in particular, in treating cancer and hemoglobinopathies. 

2-(hetero)aryl-benzimidazole and imidazopyridine derivatives as inhibitors of asparagime emethyl transferase

A compound of the formula (I): where Ror Ris a cyclic amine group and Ris an aromatic group with a carbonyl containing substituent for use as a FAK inhibitor.

FAK inhibitors

A compound of the formula (I): where Ror Ris a cycle, amine group and Ris an aromatic group with a carbonyl containing substituent for use as a FAK inhibitor.

Selective FAK inhibitors

A compound of the formula (I): where Ror Ris a cyclc amine group and Ris an aromatic group with a carbonyl containing substituent for use as a FAK inhibitor.

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Parkville, Australia

Scott Raymond Walker