AR084083A1 - Derivados de pirrolo[2,3-b]piridina sustituidos con 3-hetarilo como inhibidores de pdk1 - Google Patents

Derivados de pirrolo[2,3-b]piridina sustituidos con 3-hetarilo como inhibidores de pdk1

Info

Publication number
AR084083A1
AR084083A1 ARP110104498A ARP110104498A AR084083A1 AR 084083 A1 AR084083 A1 AR 084083A1 AR P110104498 A ARP110104498 A AR P110104498A AR P110104498 A ARP110104498 A AR P110104498A AR 084083 A1 AR084083 A1 AR 084083A1
Authority
AR
Argentina
Prior art keywords
atoms
hal
mono
replaced
nr5so2a
Prior art date
Application number
ARP110104498A
Other languages
English (en)
Inventor
Buchstaller Hans Dr
Wucherer-Plietker Margarita Peter-Dra
Heinrich Timo Dr
Original Assignee
Merck Patent Gmbh
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 filed Critical Merck Patent Gmbh
Publication of AR084083A1 publication Critical patent/AR084083A1/es

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04—Ortho-condensed systems
    • 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
    • A61K31/4353—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 ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/437—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 ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
    • 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
    • A61K31/50—Pyridazines; Hydrogenated pyridazines
    • A61K31/501—Pyridazines; Hydrogenated pyridazines not condensed and containing further heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61N—ELECTROTHERAPY; MAGNETOTHERAPY; RADIATION THERAPY; ULTRASOUND THERAPY
    • A61N5/00—Radiation therapy
    • A61N5/10—X-ray therapy; Gamma-ray therapy; Particle-irradiation therapy
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • A61P31/14—Antivirals for RNA viruses
    • A61P31/18—Antivirals for RNA viruses for HIV
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A61P35/02—Antineoplastic agents specific for leukemia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A61P35/04—Antineoplastic agents specific for metastasis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A61P37/04—Immunostimulants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00

Abstract

Son inhibidores de PDK1 y se pueden emplear para el tratamiento de tumores.Reivindicación 1: Compuestos de la fórmula (1), en donde Q es Het-diílo; R1 es Br, Het1 o fenilo monosustituido con CH2OH; R2, R3 son, de modo independiente entre sí, H, Hal, A, Ar, [C(R5)2]nOH, [C(R5)2]nOA o [C(R5)2]nN(R5)2; R2, R3 también son juntos =O, =CH2 o una cadena de alquileno con 2-5 átomos de C; R4 es H, Ar o Het2; R5 es H o A’; Het1 es pirazolilo que puede estar monosustituido con A, CH2OH, (CH2)2OH, COOH, CH2COHet3, COOA o CONH2; Ar es fenilo, naftilo o bifenilo no sustituido o mono-, di- o trisustituido con Hal, A, (CH2)nOR5, (CH2)nN(R5)2, SR5, NO2, COOR5, CON(R5)2, NR5COA, NR5SO2A, SO2N(R5)2, COR5, (CH2)nCN y/o S(O)mA; Het es un heterociclo saturado, insaturado o aromático mono- o bicíclico no sustituido o mono- o disustituido con Hal, A, [C(R5)2]nOR5, [C(R5)2]nN(R5)2, NO2, CN, COOR5, CON(R5)2, NR5COA, NR5SO2A, COR5, SO2NR5, S(O)mA, =S, =NH, =NA y/u =O (oxígeno del carbonilo) con 1 a 4 átomos de N, y/u O y/o S; Het2 es un heterociclo saturado, insaturado o aromático monocíclico no sustituido o mono- o disustituido con Hal, A, OR5, N(R5)2, NO2, CN, COOR5, CON(R5)2, NR5COA, NR5SO2A, COR5, SO2NR5, S(O)mA, =S, =NH, =NA y/u =O (oxígeno del carbonilo) con 1 a 4 átomos de N, y/u O y/o S; Het3 es un heterociclo saturado monocíclico no sustituido con 1 a 4 átomos de N, y/u O y/o S; A es alquilo no ramificado o ramificado con 1-10 átomos de C, en donde 1-7 átomos de H pueden estar reemplazados por F, Cl y/o Br, y/o en donde uno o dos grupos no adyacentes CH y/o CH2 pueden estar reemplazados por NR5, O, S, SO, SO2, CºC y/o grupos CH=CH, o alquilo cíclico con 3-7 átomos de C; A’ es alquilo no ramificado o ramificado con 1-6 átomos de C, o alquilo cíclico con 3-7 átomos de C; Hal es F, Cl, Br o l; m es 0, 1 ó 2; n es 0, 1, 2, 3 ó 4; así como sus sales, tautómeros y estereoisómeros farmacéuticamente aceptables, incluyendo sus mezclas en todas las proporciones.
ARP110104498A 2010-12-03 2011-12-02 Derivados de pirrolo[2,3-b]piridina sustituidos con 3-hetarilo como inhibidores de pdk1 AR084083A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
DE102010053347A DE102010053347A1 (de) 2010-12-03 2010-12-03 3-Hetaryl-substituierte Pyrrolo[2,3-b] pyridin-derivative als PDK1-Inhibitoren

Publications (1)

Publication Number Publication Date
AR084083A1 true AR084083A1 (es) 2013-04-17

Family

ID=45047712

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP110104498A AR084083A1 (es) 2010-12-03 2011-12-02 Derivados de pirrolo[2,3-b]piridina sustituidos con 3-hetarilo como inhibidores de pdk1

Country Status (9)

Country Link
US (1) US20130245355A1 (es)
EP (1) EP2646438A1 (es)
JP (1) JP2013544264A (es)
CN (1) CN103228657A (es)
AR (1) AR084083A1 (es)
AU (1) AU2011335450A1 (es)
CA (1) CA2819518A1 (es)
DE (1) DE102010053347A1 (es)
WO (1) WO2012072200A1 (es)

Families Citing this family (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE102011009961A1 (de) 2011-02-01 2012-08-02 Merck Patent Gmbh 7-Azaindolderivate
CN104860898B (zh) * 2014-02-25 2017-11-28 沈阳药科大学 3‑芳基噁二唑类化合物及其用途
US20170298055A1 (en) 2014-09-17 2017-10-19 Ironwood Pharmaceuticals, Inc. sGC STIMULATORS
EP3325100A4 (en) 2015-07-17 2019-02-20 Memorial Sloan-Kettering Cancer Center COMBINED THERAPY USING PDK1 AND PI3K INHIBITORS
WO2022213335A1 (en) * 2021-04-09 2022-10-13 Beigene (Beijing) Co., Ltd. Method for preparing intermediate of bcl-2 inhibitor

Family Cites Families (13)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5747469A (en) 1991-03-06 1998-05-05 Board Of Regents, The University Of Texas System Methods and compositions comprising DNA damaging agents and p53
GB9904387D0 (en) 1999-02-25 1999-04-21 Pharmacia & Upjohn Spa Antitumour synergistic composition
GB0308466D0 (en) 2003-04-11 2003-05-21 Novartis Ag Organic compounds
US7709645B2 (en) * 2004-07-27 2010-05-04 Sgx Pharmaceuticals, Inc. Pyrrolo-pyridine kinase modulators
GB0702265D0 (en) * 2007-02-06 2007-03-14 Eisai London Res Lab Ltd 7-Azaindole derivatives
GB0702259D0 (en) * 2007-02-06 2007-03-14 Eisai London Res Lab Ltd 7-azaindole derivatives
DE102007028515A1 (de) * 2007-06-21 2008-12-24 Merck Patent Gmbh 6-(Pyrrolopyridinyl)-pyrimidinyl-2-amin-derivate
WO2009054941A1 (en) * 2007-10-25 2009-04-30 Merck & Co., Inc. Therapeutic compounds
DE102008031517A1 (de) * 2008-07-03 2010-01-07 Merck Patent Gmbh Pyrrolopyridinyl-pyrimidin-2-yl-amin-derivate
DE102009019962A1 (de) * 2009-05-05 2010-11-11 Merck Patent Gmbh 3-([1,2,3]Triazol-4-yl)-pyrrolo[2,3-b]pyridinderivate
DE102009060174A1 (de) * 2009-12-23 2011-06-30 Merck Patent GmbH, 64293 Pyrrolopyridinyl-pyrimidin-2-yl-amin-derivate
DE102010050558A1 (de) * 2010-11-05 2012-05-10 Merck Patent Gmbh 1H-Pyrrolo[2,3-b]pyridinderivate
DE102011009961A1 (de) * 2011-02-01 2012-08-02 Merck Patent Gmbh 7-Azaindolderivate

Also Published As

Publication number Publication date
CN103228657A (zh) 2013-07-31
CA2819518A1 (en) 2012-06-07
EP2646438A1 (de) 2013-10-09
JP2013544264A (ja) 2013-12-12
AU2011335450A1 (en) 2013-07-18
WO2012072200A1 (de) 2012-06-07
DE102010053347A1 (de) 2012-06-06
US20130245355A1 (en) 2013-09-19

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