WO2001044161A3 - Verfahren zur herstellung kombinatorischer bibliotheken arylsubstituierter amine - Google Patents

Verfahren zur herstellung kombinatorischer bibliotheken arylsubstituierter amine Download PDF

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Publication number
WO2001044161A3
WO2001044161A3 PCT/EP2000/012173 EP0012173W WO0144161A3 WO 2001044161 A3 WO2001044161 A3 WO 2001044161A3 EP 0012173 W EP0012173 W EP 0012173W WO 0144161 A3 WO0144161 A3 WO 0144161A3
Authority
WO
WIPO (PCT)
Prior art keywords
aryl
substituted amines
combinatorial libraries
producing combinatorial
libraries
Prior art date
Application number
PCT/EP2000/012173
Other languages
English (en)
French (fr)
Other versions
WO2001044161A2 (de
Inventor
Herwig Buchholz
Urs Welz-Biermann
Original Assignee
Merck Patent Gmbh
Herwig Buchholz
Welz Biermann Urs
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 Merck Patent Gmbh, Herwig Buchholz, Welz Biermann Urs filed Critical Merck Patent Gmbh
Priority to AU30058/01A priority Critical patent/AU3005801A/en
Publication of WO2001044161A2 publication Critical patent/WO2001044161A2/de
Publication of WO2001044161A3 publication Critical patent/WO2001044161A3/de

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D295/00—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms
    • C07D295/02—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms containing only hydrogen and carbon atoms in addition to the ring hetero elements
    • C07D295/027—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms containing only hydrogen and carbon atoms in addition to the ring hetero elements containing only one hetero ring
    • C07D295/03—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms containing only hydrogen and carbon atoms in addition to the ring hetero elements containing only one hetero ring with the ring nitrogen atoms directly attached to acyclic carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C209/00—Preparation of compounds containing amino groups bound to a carbon skeleton
    • C07C209/68—Preparation of compounds containing amino groups bound to a carbon skeleton from amines, by reactions not involving amino groups, e.g. reduction of unsaturated amines, aromatisation, or substitution of the carbon skeleton
    • C07C209/76—Preparation of compounds containing amino groups bound to a carbon skeleton from amines, by reactions not involving amino groups, e.g. reduction of unsaturated amines, aromatisation, or substitution of the carbon skeleton by nitration
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C211/00—Compounds containing amino groups bound to a carbon skeleton
    • C07C211/01—Compounds containing amino groups bound to a carbon skeleton having amino groups bound to acyclic carbon atoms
    • C07C211/26—Compounds containing amino groups bound to a carbon skeleton having amino groups bound to acyclic carbon atoms of an unsaturated carbon skeleton containing at least one six-membered aromatic ring
    • C07C211/27—Compounds containing amino groups bound to a carbon skeleton having amino groups bound to acyclic carbon atoms of an unsaturated carbon skeleton containing at least one six-membered aromatic ring having amino groups linked to the six-membered aromatic ring by saturated carbon chains
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C211/00—Compounds containing amino groups bound to a carbon skeleton
    • C07C211/01—Compounds containing amino groups bound to a carbon skeleton having amino groups bound to acyclic carbon atoms
    • C07C211/26—Compounds containing amino groups bound to a carbon skeleton having amino groups bound to acyclic carbon atoms of an unsaturated carbon skeleton containing at least one six-membered aromatic ring
    • C07C211/28—Compounds containing amino groups bound to a carbon skeleton having amino groups bound to acyclic carbon atoms of an unsaturated carbon skeleton containing at least one six-membered aromatic ring having amino groups linked to the six-membered aromatic ring by unsaturated carbon chains
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C211/00—Compounds containing amino groups bound to a carbon skeleton
    • C07C211/01—Compounds containing amino groups bound to a carbon skeleton having amino groups bound to acyclic carbon atoms
    • C07C211/26—Compounds containing amino groups bound to a carbon skeleton having amino groups bound to acyclic carbon atoms of an unsaturated carbon skeleton containing at least one six-membered aromatic ring
    • C07C211/29—Compounds containing amino groups bound to a carbon skeleton having amino groups bound to acyclic carbon atoms of an unsaturated carbon skeleton containing at least one six-membered aromatic ring the carbon skeleton being further substituted by halogen atoms or by nitro or nitroso groups
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C211/00—Compounds containing amino groups bound to a carbon skeleton
    • C07C211/43—Compounds containing amino groups bound to a carbon skeleton having amino groups bound to carbon atoms of six-membered aromatic rings of the carbon skeleton
    • C07C211/44—Compounds containing amino groups bound to a carbon skeleton having amino groups bound to carbon atoms of six-membered aromatic rings of the carbon skeleton having amino groups bound to only one six-membered aromatic ring
    • C07C211/45—Monoamines
    • C07C211/48—N-alkylated amines
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C217/00—Compounds containing amino and etherified hydroxy groups bound to the same carbon skeleton
    • C07C217/54—Compounds containing amino and etherified hydroxy groups bound to the same carbon skeleton having etherified hydroxy groups bound to carbon atoms of at least one six-membered aromatic ring and amino groups bound to acyclic carbon atoms or to carbon atoms of rings other than six-membered aromatic rings of the same carbon skeleton
    • C07C217/56—Compounds containing amino and etherified hydroxy groups bound to the same carbon skeleton having etherified hydroxy groups bound to carbon atoms of at least one six-membered aromatic ring and amino groups bound to acyclic carbon atoms or to carbon atoms of rings other than six-membered aromatic rings of the same carbon skeleton with amino groups linked to the six-membered aromatic ring, or to the condensed ring system containing that ring, by carbon chains not further substituted by singly-bound oxygen atoms
    • C07C217/58—Compounds containing amino and etherified hydroxy groups bound to the same carbon skeleton having etherified hydroxy groups bound to carbon atoms of at least one six-membered aromatic ring and amino groups bound to acyclic carbon atoms or to carbon atoms of rings other than six-membered aromatic rings of the same carbon skeleton with amino groups linked to the six-membered aromatic ring, or to the condensed ring system containing that ring, by carbon chains not further substituted by singly-bound oxygen atoms with amino groups and the six-membered aromatic ring, or the condensed ring system containing that ring, bound to the same carbon atom of the carbon chain
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D295/00—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms
    • C07D295/04—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms
    • C07D295/06—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by halogen atoms or nitro radicals
    • C07D295/073—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by halogen atoms or nitro radicals with the ring nitrogen atoms and the substituents separated by carbocyclic rings or by carbon chains interrupted by carbocyclic rings
    • C—CHEMISTRY; METALLURGY
    • C40—COMBINATORIAL TECHNOLOGY
    • C40B—COMBINATORIAL CHEMISTRY; LIBRARIES, e.g. CHEMICAL LIBRARIES
    • C40B40/00—Libraries per se, e.g. arrays, mixtures

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)

Abstract

Die vorliegende Erfindung betrifft ein Verfahren zur Herstellung kombinatorischer Bibliotheken arylsubstituierter Amine umfassend mindestens zwei verschiedene Verbindungen der allgemeinen Formel (I). Insbesondere betrifft die vorliegende Erfindung Bibliotheken geminal substituierter Amine, welche mindestens einen eine Arylgruppe aufweisenden Substituenten R?4 oder R5¿ besitzen, sowie die spezielle Verwendung dieser Amine als Zwischenstufen in der kombinatorischen Wirkstoffsynthese oder als Wirkstoffe in Arzneimitteln.
PCT/EP2000/012173 1999-12-17 2000-12-04 Verfahren zur herstellung kombinatorischer bibliotheken arylsubstituierter amine WO2001044161A2 (de)

Priority Applications (1)

Application Number Priority Date Filing Date Title
AU30058/01A AU3005801A (en) 1999-12-17 2000-12-04 Method for producing combinatorial libraries of aryl-substituted amines

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
DE1999161372 DE19961372A1 (de) 1999-12-17 1999-12-17 Verfahren zur Herstellung kombinatorischer Bibliotheken arylsubstituierter Amine
DE19961372.9 1999-12-17

Publications (2)

Publication Number Publication Date
WO2001044161A2 WO2001044161A2 (de) 2001-06-21
WO2001044161A3 true WO2001044161A3 (de) 2002-04-11

Family

ID=7933367

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PCT/EP2000/012173 WO2001044161A2 (de) 1999-12-17 2000-12-04 Verfahren zur herstellung kombinatorischer bibliotheken arylsubstituierter amine

Country Status (3)

Country Link
AU (1) AU3005801A (de)
DE (1) DE19961372A1 (de)
WO (1) WO2001044161A2 (de)

Families Citing this family (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US8637706B2 (en) 2005-11-28 2014-01-28 Gtx, Inc. Nuclear receptor binding agents
US8158828B2 (en) 2005-11-28 2012-04-17 Gtx, Inc. Nuclear receptor binding agents
US8546451B2 (en) 2005-11-28 2013-10-01 Gtx, Inc. Estrogen receptor ligands and methods of use thereof
US9409856B2 (en) 2005-11-28 2016-08-09 Gtx, Inc. Estrogen receptor ligands and methods of use thereof
US9427418B2 (en) 2009-02-23 2016-08-30 Gtx, Inc. Estrogen receptor ligands and methods of use thereof
US9624161B2 (en) 2009-02-23 2017-04-18 Gtx, Inc. Estrogen receptor ligands and methods of use thereof

Citations (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB807835A (en) * 1955-07-01 1959-01-21 Thomae Gmbh Dr K New tertiary amines and their salts and process for their preparation
US4020059A (en) * 1975-06-02 1977-04-26 Nippon Shokubai Kagaku Kogyo Co., Ltd. Process for preparing tertiary amines
WO1998000398A1 (en) * 1996-06-28 1998-01-08 University Of Southern California Method for the synthesis of amines and amino acids with organoboron derivatives
EP0818431A1 (de) * 1996-06-14 1998-01-14 Eli Lilly And Company Kombinatorisches Verfahren unter Verwendung von Fängerverbindungen zur Herstellung von Bibliotheken von sekundären Aminverdindungen
WO1999065855A2 (de) * 1998-06-18 1999-12-23 Merck Patent Gmbh Kombinatorische bibliotheken geminal substituierter amine

Patent Citations (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB807835A (en) * 1955-07-01 1959-01-21 Thomae Gmbh Dr K New tertiary amines and their salts and process for their preparation
US4020059A (en) * 1975-06-02 1977-04-26 Nippon Shokubai Kagaku Kogyo Co., Ltd. Process for preparing tertiary amines
EP0818431A1 (de) * 1996-06-14 1998-01-14 Eli Lilly And Company Kombinatorisches Verfahren unter Verwendung von Fängerverbindungen zur Herstellung von Bibliotheken von sekundären Aminverdindungen
WO1998000398A1 (en) * 1996-06-28 1998-01-08 University Of Southern California Method for the synthesis of amines and amino acids with organoboron derivatives
WO1999065855A2 (de) * 1998-06-18 1999-12-23 Merck Patent Gmbh Kombinatorische bibliotheken geminal substituierter amine
WO1999065863A1 (de) * 1998-06-18 1999-12-23 Merck Patent Gmbh Verfahren zur herstellung von kombinatorischen aminbibliotheken
WO1999065864A2 (de) * 1998-06-18 1999-12-23 Merck Patent Gmbh Geminal substituierte amine

Non-Patent Citations (18)

* Cited by examiner, † Cited by third party
Title
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"BEILSTEINS HANDBUCH DER ORGANISCHEN CHEMIE, vierte Auflage, viertes Ergänzungswerk, Band XII, vierter Teil, S. 2182", BEILSTEINS HANDBUCH DER ORGANISCHEN CHEMIE,XX,XX, VOL. 12, NR. 4, PAGE(S) 2182, XP002118213 *
"HOUBEN-WEYL, METHODEN DER ORGANISCHEN CHEMIE, vol. XI/1, S. 820-823", HOUBEN-WEYL METHODEN DER ORGANISCHEN CHEMIE,DE,GEORGE THIEME VERLAG, STUTTGART, VOL. 11, NR. 1, PAGE(S) 820-823, XP002117680 *
BACHELET, JEAN-PIERRE ET AL., J. ORG. CHEM., vol. 47, no. 2, 1982, pages 234 - 8 *
BALTZLY ET AL., J. ORG. CHEM., vol. 14, 1949, pages 775, 777, 779 *
BILLMAN, TAI, J. ORG. CHEM., vol. 23, 1958, pages 535, 537, 538 *
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Publication number Publication date
WO2001044161A2 (de) 2001-06-21
AU3005801A (en) 2001-06-25
DE19961372A1 (de) 2001-06-21

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