Ctxt Pty Limited

Cancer Therapeutics Crc Pty Limited

Pfizer Corporation

Michelle Ang Camerino

Paul Anthony Stupple

Scott Raymond Walker

Richard Charles Foitzik

Benjamin Joseph Morrow

Ylva Elisabet Bergman

Ylva Elisabet Bergman Bozikis

H Rachel Lagiakos

Wilhelmus Johannes Antonius Kersten

Romina Lessene

Danny Ganame

Ian Peter Holmes

Gillian Elizabeth Lunniss

Jonathan Grant Hubert

Andrew John Harvey

Scott Channing Sutton

Pei-Pei Kung

Catherine Fae Hemley

John Feutrill

Anthony Nicholas Cuzzupe

Helen Rachel Lagiakos

Graeme Irvine Stevenson

Robert Louis Hoffman

Robert Arnold Kumpf

Paul Francis Richardson

Neil Choi

Samantha Elizabeth Greasley

Oleg Brodsky

Alexandra Elizabeth Stupple

Matthew Lloyd Dennis

Jo-Anne Pinson

George Nikolakopoulos

Ylva Elisabet Bozikis

This disclosure relates to compounds of formula (I), which are modulators of STING. Also disclosed are pharmaceutical compositions comprising compounds of formula (I) and methods of using compounds of formula (I) in the treatment or prevention of diseases ameliorated by the modulation of STING.

Compound modulators of sting

A compound of formula (I): wherein: Y is (CH2)n, where n is from 2 to 4; W1 and W11 are independently selected from OH and ORP, where RP is Me or Et.

Benzothiophene, thienopyridine and thienopyrimidine derivatives for the modulation of sting

The present invention relates to compounds of formula (I) or pharmaceutically acceptable salts thereof, wherein Ring A, R-R, and n are defined herein. The novel benzisoxazole sulfonamide derivatives are useful in the treatment of abnormal cell growth, such as cancer, in patients. Additional embodiments relate to pharmaceutical compositions containing the compounds and to methods of using the compounds and compositions in the treatment of abnormal cell growth in patients.

Benzisoxazole sulfonamide derivatives

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: (I) wherein: n is 1 or 2; p is 0 or 1; R, R, Rand Rare independently selected from H, halo, Calkyl, Cfluoroalkyl, Ccycloalkyl, Calkyloxy, 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 (IIa), where Ris selected from N-linked N-containing Cheterocycyl and (A); or (ii) (IIb), where X is selected from CH, NH and O, one of Rand Ris selected from CI and ethoxy and the other of Rand Ris H. 

Benzopiperdine derivatives and their use in the treatment of cancer and hemoglobinopathies

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; 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. 

Tetrahydroisoquinolines as PRMT5 inhibitors

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

This invention relates to compounds of the formula (I): The invention also relates to processes for the preparation of the compound of the formula (I), pharmaceutical agents or compositions containing the compound or a method of using the compound for the treatment of proliferative diseases, such as cancer, as well as the treatment of diseases ameliorated by the control and/or inhibition of lymphangiogenesis.

Growing community of inventors

Victoria, Australia

Michelle Ang Camerino