WO2006040569A8 - Thiophene amide compounds for use in the treatment or prophylaxis of cancers - Google Patents

Thiophene amide compounds for use in the treatment or prophylaxis of cancers

Info

Publication number
WO2006040569A8
WO2006040569A8 PCT/GB2005/003957 GB2005003957W WO2006040569A8 WO 2006040569 A8 WO2006040569 A8 WO 2006040569A8 GB 2005003957 W GB2005003957 W GB 2005003957W WO 2006040569 A8 WO2006040569 A8 WO 2006040569A8
Authority
WO
WIPO (PCT)
Prior art keywords
optionally substituted
group
prophylaxis
treatment
compound
Prior art date
Application number
PCT/GB2005/003957
Other languages
French (fr)
Other versions
WO2006040569A1 (en
Inventor
Adrian Liam Gill
John Francis Lyons
Neil Thomas Thompson
Original Assignee
Astex Therapeutics Ltd
Adrian Liam Gill
John Francis Lyons
Neil Thomas Thompson
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Astex Therapeutics Ltd, Adrian Liam Gill, John Francis Lyons, Neil Thomas Thompson filed Critical Astex Therapeutics Ltd
Publication of WO2006040569A1 publication Critical patent/WO2006040569A1/en
Publication of WO2006040569A8 publication Critical patent/WO2006040569A8/en

Links

Classifications

    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/415—1,2-Diazoles
    • A61K31/4155—1,2-Diazoles non condensed and containing further heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/4439—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/496—Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/5375—1,4-Oxazines, e.g. morpholine
    • A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/5375—1,4-Oxazines, e.g. morpholine
    • A61K31/5386—1,4-Oxazines, e.g. morpholine spiro-condensed or forming part of bridged ring systems
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents

Abstract

The invention provides the use of a compound for the manufacture of a medicament for the prophylaxis or treatment of a cancer or a para-neoplastic effect associated with a cancer, the para-neoplastic effect being other than cachexia, and the compound being a compound of the formula (I), or a salt, solvate or N-oxide thereof, wherein: R1 and R2 are the same or different and each is selected from hydrogen, C1-4 hydrocarbyl, halogen and cyano; X is selected from C=O, C=S, C(=O)NH, C(=S)NH, C(=O)O, C(=O)S, C(=S)O and C(=S)S; R3 is an aryl or heteroaryl group of 5 to 12 ring members optionally substituted by one or more substituent groups R7 wherein R7 is as defined in the claims; R4 is a group YR5 or a group R6; Y is NH, O or S; R5 is selected from (a) optionally substituted carbocyclic and heterocyclic groups having from 3 to 12 ring members; and (b) optionally substituted C1-8 hydrocarbyl 20 groups; and R6 is an optionally substituted heterocyclic group having from 4 to 12 ring members and containing at least one ring nitrogen atom through which R6 is linked to the adjacent carbonyl group.
PCT/GB2005/003957 2004-10-14 2005-10-14 Thiophene amide compounds for use in the treatment or prophylaxis of cancers WO2006040569A1 (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US61878004P 2004-10-14 2004-10-14
US60/618,780 2004-10-14

Publications (2)

Publication Number Publication Date
WO2006040569A1 WO2006040569A1 (en) 2006-04-20
WO2006040569A8 true WO2006040569A8 (en) 2007-04-26

Family

ID=35502547

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/GB2005/003957 WO2006040569A1 (en) 2004-10-14 2005-10-14 Thiophene amide compounds for use in the treatment or prophylaxis of cancers

Country Status (1)

Country Link
WO (1) WO2006040569A1 (en)

Families Citing this family (14)

* Cited by examiner, † Cited by third party
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KR20080103996A (en) 2006-02-16 2008-11-28 쉐링 코포레이션 Pyrrolidine derivatives as erk inhibitors
JP4884072B2 (en) * 2006-05-12 2012-02-22 三井化学アグロ株式会社 Heterocyclic derivatives and their use as insecticides
RU2525389C2 (en) 2008-02-21 2014-08-10 Мерк Шарп И Доум Корп. Compounds which are erk inhibitors
EP2297097A2 (en) * 2008-06-11 2011-03-23 Irm Llc Compounds and compositions useful for the treatment of malaria
FR2945289A1 (en) 2009-05-11 2010-11-12 Sanofi Aventis 2-CYCLOAMINO-5- (PYRIDIN-4-YL) IMIDAZO-2,1-B1 DERIVATIVES 1,3,4! THIADIAZOLE, THEIR PREPARATION AND THEIR THERAPEUTIC APPLICATION
US9408885B2 (en) 2011-12-01 2016-08-09 Vib Vzw Combinations of therapeutic agents for treating melanoma
WO2014043633A1 (en) 2012-09-17 2014-03-20 Agios Pharmaceuticals, Inc. Use of e-cadherin and vimentin for selection of treatment responsive patients
US10011574B2 (en) 2012-11-21 2018-07-03 Agios Pharmaceuticals, Inc. Glutaminase inhibitors and method of use
WO2014079011A1 (en) 2012-11-22 2014-05-30 Agios Pharmaceuticals, Inc. Heterocyclic compounds for inhibiting glutaminase and their methods of use
KR20160127149A (en) * 2014-03-21 2016-11-02 아지오스 파마슈티컬스 아이엔씨. Compounds and Their Methods of Use
WO2017117532A1 (en) * 2015-12-31 2017-07-06 Cantley Lewis C Small molecule inhibitor of 3-phosphoglycerate dehydrogenase and uses thereof
EP3579872A1 (en) 2017-02-10 2019-12-18 INSERM (Institut National de la Santé et de la Recherche Médicale) Methods and pharmaceutical compositions for the treatment of cancers associated with activation of the mapk pathway
CA3086765A1 (en) 2017-12-28 2019-07-04 Tract Pharmaceuticals, Inc. Stem cell culture systems for columnar epithelial stem cells, and uses related thereto
EP3801504A4 (en) * 2018-06-11 2022-07-27 Northeastern University Selective ligands for modulation of girk channels

Family Cites Families (12)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
IT1196390B (en) * 1984-12-28 1988-11-16 Consiglio Nazionale Ricerche New pharmaceutical compsns. useful in tumour therapy
US6187799B1 (en) * 1997-05-23 2001-02-13 Onyx Pharmaceuticals Inhibition of raf kinase activity using aryl ureas
US6037340A (en) * 1997-05-28 2000-03-14 Cadus Pharmaceutical Corporation Synthesis and use of thiophene- and pyrrole-based heteroaromatic compounds
WO2001025190A1 (en) * 1999-10-01 2001-04-12 Japan Energy Corporation Novel diarylamide derivatives and use thereof as medicines
US6414013B1 (en) * 2000-06-19 2002-07-02 Pharmacia & Upjohn S.P.A. Thiophene compounds, process for preparing the same, and pharmaceutical compositions containing the same background of the invention
JP2003267869A (en) * 2002-03-13 2003-09-25 Toray Ind Inc Thiophene derivative- or indole derivative-containing medicine
JP2005531608A (en) * 2002-06-06 2005-10-20 スミスクライン・ビーチャム・コーポレイション NF-κB inhibitor
US7196106B2 (en) * 2002-11-05 2007-03-27 Merck & Co., Inc Cyanothiophene derivatives, compositions containing such compounds and methods of use
GB0308511D0 (en) * 2003-04-14 2003-05-21 Astex Technology Ltd Pharmaceutical compounds
US20050085531A1 (en) * 2003-10-03 2005-04-21 Hodge Carl N. Thiophene-based compounds exhibiting ATP-utilizing enzyme inhibitory activity, and compositions, and uses thereof
JP2007508318A (en) * 2003-10-09 2007-04-05 エートン ファーマ インコーポレーティッド Thiophene and benzothiophene hydroxamic acid derivatives
WO2005100338A1 (en) * 2004-04-13 2005-10-27 Astex Therapeutics Limited 5-morpholinylmethylthiophenyl pharmaceutial compounds as p38 map kinase modulators

Also Published As

Publication number Publication date
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