WO2005023794A3 - Compound libraries of 4-carboxamidopiperidine derivatives - Google Patents

Compound libraries of 4-carboxamidopiperidine derivatives Download PDF

Info

Publication number
WO2005023794A3
WO2005023794A3 PCT/GB2004/003850 GB2004003850W WO2005023794A3 WO 2005023794 A3 WO2005023794 A3 WO 2005023794A3 GB 2004003850 W GB2004003850 W GB 2004003850W WO 2005023794 A3 WO2005023794 A3 WO 2005023794A3
Authority
WO
WIPO (PCT)
Prior art keywords
carboxamidopiperidine
derivatives
library
compound libraries
designed
Prior art date
Application number
PCT/GB2004/003850
Other languages
French (fr)
Other versions
WO2005023794A2 (en
Inventor
Graham Peter Jones
Jacqueline Anne Macritchie
Martin John Slater
Original Assignee
Biofocus Plc
Graham Peter Jones
Jacqueline Anne Macritchie
Martin John Slater
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 Biofocus Plc, Graham Peter Jones, Jacqueline Anne Macritchie, Martin John Slater filed Critical Biofocus Plc
Publication of WO2005023794A2 publication Critical patent/WO2005023794A2/en
Publication of WO2005023794A3 publication Critical patent/WO2005023794A3/en

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C04—CEMENTS; CONCRETE; ARTIFICIAL STONE; CERAMICS; REFRACTORIES
    • C04B—LIME, MAGNESIA; SLAG; CEMENTS; COMPOSITIONS THEREOF, e.g. MORTARS, CONCRETE OR LIKE BUILDING MATERIALS; ARTIFICIAL STONE; CERAMICS; REFRACTORIES; TREATMENT OF NATURAL STONE
    • C04B35/00—Shaped ceramic products characterised by their composition; Ceramics compositions; Processing powders of inorganic compounds preparatory to the manufacturing of ceramic products
    • C04B35/622—Forming processes; Processing powders of inorganic compounds preparatory to the manufacturing of ceramic products
    • C04B35/626—Preparing or treating the powders individually or as batches ; preparing or treating macroscopic reinforcing agents for ceramic products, e.g. fibres; mechanical aspects section B
    • C04B35/63—Preparing or treating the powders individually or as batches ; preparing or treating macroscopic reinforcing agents for ceramic products, e.g. fibres; mechanical aspects section B using additives specially adapted for forming the products, e.g.. binder binders
    • C04B35/632—Organic additives
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D211/00—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
    • C07D211/04—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D211/06—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
    • C07D211/36—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D211/40—Oxygen atoms
    • C07D211/44—Oxygen atoms attached in position 4
    • C07D211/46—Oxygen atoms attached in position 4 having a hydrogen atom as the second substituent in position 4
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D211/00—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
    • C07D211/04—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D211/06—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
    • C07D211/36—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D211/56—Nitrogen atoms
    • C07D211/58—Nitrogen atoms attached in position 4
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/24—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with substituted hydrocarbon radicals attached to ring carbon atoms
    • C07D213/36—Radicals substituted by singly-bound nitrogen atoms
    • C07D213/38—Radicals substituted by singly-bound nitrogen atoms having only hydrogen or hydrocarbon radicals attached to the substituent nitrogen atom
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C40—COMBINATORIAL TECHNOLOGY
    • C40B—COMBINATORIAL CHEMISTRY; LIBRARIES, e.g. CHEMICAL LIBRARIES
    • C40B40/00—Libraries per se, e.g. arrays, mixtures
    • C40B40/04—Libraries containing only organic compounds
    • C—CHEMISTRY; METALLURGY
    • C40—COMBINATORIAL TECHNOLOGY
    • C40B—COMBINATORIAL CHEMISTRY; LIBRARIES, e.g. CHEMICAL LIBRARIES
    • C40B50/00—Methods of creating libraries, e.g. combinatorial synthesis
    • C40B50/08—Liquid phase synthesis, i.e. wherein all library building blocks are in liquid phase or in solution during library creation; Particular methods of cleavage from the liquid support

Abstract

The present invention provides a compound library targeted to receptors that recognise a central secondary amide moiety. The library is designed around an acetamide coupled to a piperidine moiety. A combination of specific motifs R1, R2, R3, and R4 are appended from the central scaffold and are designed to pick up different interactions at a receptor site. The library comprises or consists of a set of structurally related compounds of general formula (II).
PCT/GB2004/003850 2003-09-08 2004-09-08 Compound libraries of 4-carboxamidopiperidine derivatives WO2005023794A2 (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
GB0320983A GB0320983D0 (en) 2003-09-08 2003-09-08 Compound libraries
GB0320983.0 2003-09-08

Publications (2)

Publication Number Publication Date
WO2005023794A2 WO2005023794A2 (en) 2005-03-17
WO2005023794A3 true WO2005023794A3 (en) 2005-06-02

Family

ID=29226682

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/GB2004/003850 WO2005023794A2 (en) 2003-09-08 2004-09-08 Compound libraries of 4-carboxamidopiperidine derivatives

Country Status (2)

Country Link
GB (1) GB0320983D0 (en)
WO (1) WO2005023794A2 (en)

Families Citing this family (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP2723718A1 (en) 2011-06-24 2014-04-30 Amgen Inc. Trpm8 antagonists and their use in treatments
PE20140868A1 (en) 2011-06-24 2014-07-18 Amgen Inc TRPM8 ANTAGONISTS AND THEIR USE IN TREATMENTS
US8952009B2 (en) 2012-08-06 2015-02-10 Amgen Inc. Chroman derivatives as TRPM8 inhibitors
US10633336B2 (en) 2014-12-19 2020-04-28 The Broad Institute, Inc. Dopamine D2 receptor ligands
EP3233799B1 (en) 2014-12-19 2021-05-19 The Broad Institute, Inc. Dopamine d2 receptor ligands

Citations (9)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE2415063A1 (en) * 1974-03-28 1975-10-16 Bayer Ag Pyridyl alkyl-amidine derivs - hypoglycemics which influence flat metabolism for use in diabetes, hyperlipemia and adiposis
US5516783A (en) * 1992-02-11 1996-05-14 British Biotech Pharmaceuticals Limited 4-(1H-2-methylimidazo[4,5-c]pyridinylmethyl)phenylsulphonamide derivatives as antagonist of PAF
WO1999003832A1 (en) * 1997-07-14 1999-01-28 Phytera Symbion Aps Piperidine oligomers and combinatorial libraries thereof
WO2000001375A2 (en) * 1998-06-30 2000-01-13 Neuromed Technologies, Inc. Calcium channel blockers
WO2001064632A1 (en) * 2000-03-03 2001-09-07 Aventis Pharma S.A. Azetidine derivatives, preparation thereof and pharmaceutical compositions containing same
WO2002022572A2 (en) * 2000-09-11 2002-03-21 Sepracor, Inc. Ligands for monoamine receptors and transporters, and methods of use thereof (neurotransmission)
WO2002083624A1 (en) * 2001-04-16 2002-10-24 Schering Corporation 3,4-di-substituted cyclobutene-1,2-diones as cxc-chemokine receptor ligands
WO2004058755A2 (en) * 2002-12-24 2004-07-15 Biofocus Plc Compound libraries of imidazo[1,5-a]pyridin-3-yl derivatives and related heterobicycles for targetting compounds capable of binding to g-protein coupled receptors
WO2004058259A1 (en) * 2002-12-24 2004-07-15 Biofocus Plc Compound libraries of n-(aminocarbonyl)-piperidine-4-carboxamide derivatives capable of binding to g-protein coupled receptors

Patent Citations (9)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE2415063A1 (en) * 1974-03-28 1975-10-16 Bayer Ag Pyridyl alkyl-amidine derivs - hypoglycemics which influence flat metabolism for use in diabetes, hyperlipemia and adiposis
US5516783A (en) * 1992-02-11 1996-05-14 British Biotech Pharmaceuticals Limited 4-(1H-2-methylimidazo[4,5-c]pyridinylmethyl)phenylsulphonamide derivatives as antagonist of PAF
WO1999003832A1 (en) * 1997-07-14 1999-01-28 Phytera Symbion Aps Piperidine oligomers and combinatorial libraries thereof
WO2000001375A2 (en) * 1998-06-30 2000-01-13 Neuromed Technologies, Inc. Calcium channel blockers
WO2001064632A1 (en) * 2000-03-03 2001-09-07 Aventis Pharma S.A. Azetidine derivatives, preparation thereof and pharmaceutical compositions containing same
WO2002022572A2 (en) * 2000-09-11 2002-03-21 Sepracor, Inc. Ligands for monoamine receptors and transporters, and methods of use thereof (neurotransmission)
WO2002083624A1 (en) * 2001-04-16 2002-10-24 Schering Corporation 3,4-di-substituted cyclobutene-1,2-diones as cxc-chemokine receptor ligands
WO2004058755A2 (en) * 2002-12-24 2004-07-15 Biofocus Plc Compound libraries of imidazo[1,5-a]pyridin-3-yl derivatives and related heterobicycles for targetting compounds capable of binding to g-protein coupled receptors
WO2004058259A1 (en) * 2002-12-24 2004-07-15 Biofocus Plc Compound libraries of n-(aminocarbonyl)-piperidine-4-carboxamide derivatives capable of binding to g-protein coupled receptors

Non-Patent Citations (4)

* Cited by examiner, † Cited by third party
Title
"Laborchemikalien und analytische Reagenzien", 1999, FLUKA RIEDEL-DE HAEN, XP002304990 *
A.K. DUTTA ET AL.: "Structure-Activity Relationship Studies of 4-[2-(Diphenylmethoxy)ethyl]-1-benzylpiperidine Derivatives and Their N-Analogues: Evaluation of Behavioral Activity of O- and N-Analogues and Their Binding to Monoamine Transporters", J. MED. CHEM., vol. 44, no. 6, 2001, pages 937-948, XP002304988 *
E.M. ROBERTS: "Naphthylalkyl Lactamimides as Inhibitos of Blood Platelet Aggregation", J. MED. CHEM., vol. 15, no. 12, 1972, pages 1270 - 1273, XP002304989 *
K. SHIMADA ET AL.: "Synthesis and Gastric Antisecretory Activity of N-Cyano-N'-(phenyl-pyridinylmethyl)guanidine Derivatives", CHEM. PHARM. BULL., vol. 32, no. 12, 1984, pages 4893 - 4906, XP001203593 *

Also Published As

Publication number Publication date
WO2005023794A2 (en) 2005-03-17
GB0320983D0 (en) 2003-10-08

Similar Documents

Publication Publication Date Title
WO2004000808A3 (en) N-substituted piperidine derivatives as serotonin receptor agents
NO20020214L (en) Substituted oxoazaheterocyclyl compounds
MY141559A (en) Triazole derivatives as tachykinin receptor antagonists
MY141255A (en) Phosphodiesterase 4 inhibitors, including n-substituted diarylamine analogs
HRP20080666T3 (en) Cgrp receptor antagonists
HUP0400326A2 (en) N-aroyl cyclic amine derivatives as orexin receptor antagonists
WO2002074726A3 (en) Aniline derivatives useful as phosphodiesterase 4 inhibitors
NO20030154L (en) N-oxides as NKI receptor antagonist prodrugs of 4-phenylpyridine derivatives
EP1400518A4 (en) Heterocyclic compound derivatives and medicines
UY27597A1 (en) ACRIDONA INHIBITORS OF THE IMPDH ENZYME
DE60130771D1 (en) SUBSTITUTED HETEROCYCLIC AMIDS
MY135686A (en) Indole derivatives useful as histamine h3 antagonists
ATE491703T1 (en) PHTHALAZINONE DERIVATIVES
ATE218139T1 (en) XANTHINE DERIVATIVES
WO2004046113A3 (en) Pyridine n-oxide compounds as phosphodiesterase 4 inhibitors
EP1338594A4 (en) Pgd2 receptor antagonistic pharmaceutical compositions
NO20061832L (en) Carbamide derivatives of amide type
MY138826A (en) 2,7-substituted indoles
WO2008076247A3 (en) Nitroderivatives as angiotensin ii receptor antagonists
WO2005023794A3 (en) Compound libraries of 4-carboxamidopiperidine derivatives
ATE453389T1 (en) CERTAIN PHARMACEUTICALLY VALUABLE SUBSTITUTED AMINOALKYL HETEROCYCLES
WO2004091627A3 (en) Heterocyclic substituted 1,4-dihydro-4-oxo-1,8-naphthpyridine analogs
DK1255745T3 (en) Synthesis of water-soluble 9-dihydro-paclitaxel derivatives from 9-dihydro-13-acetylbaccatin III
WO2004099130A3 (en) 1,2-diarylimidazoles useful as inhibitors of cox
MY139258A (en) Carbamoyl-type benzofuran derivatives

Legal Events

Date Code Title Description
AK Designated states

Kind code of ref document: A2

Designated state(s): AE AG AL AM AT AU AZ BA BB BG BR BW BY BZ CA CH CN CO CR CU CZ DE DK DM DZ EC EE EG ES FI GB GD GE GH GM HR HU ID IL IN IS JP KE KG KP KR KZ LC LK LR LS LT LU LV MA MD MG MK MN MW MX MZ NA NI NO NZ OM PG PH PL PT RO RU SC SD SE SG SK SL SY TJ TM TN TR TT TZ UA UG US UZ VC VN YU ZA ZM ZW

AL Designated countries for regional patents

Kind code of ref document: A2

Designated state(s): GM KE LS MW MZ NA SD SL SZ TZ UG ZM ZW AM AZ BY KG KZ MD RU TJ TM AT BE BG CH CY CZ DE DK EE ES FI FR GB GR HU IE IT LU MC NL PL PT RO SE SI SK TR BF BJ CF CG CI CM GA GN GQ GW ML MR NE SN TD TG

121 Ep: the epo has been informed by wipo that ep was designated in this application
122 Ep: pct application non-entry in european phase