WO2014207573A8 - Brustkrebszellwachstum-hemmende enzyminhibitoren, verfahren zu ihrer herstellung sowie deren verwendung - Google Patents

Brustkrebszellwachstum-hemmende enzyminhibitoren, verfahren zu ihrer herstellung sowie deren verwendung Download PDF

Info

Publication number
WO2014207573A8
WO2014207573A8 PCT/IB2014/002141 IB2014002141W WO2014207573A8 WO 2014207573 A8 WO2014207573 A8 WO 2014207573A8 IB 2014002141 W IB2014002141 W IB 2014002141W WO 2014207573 A8 WO2014207573 A8 WO 2014207573A8
Authority
WO
WIPO (PCT)
Prior art keywords
breast cancer
enzyme inhibitors
aggressive breast
cell growth
developed
Prior art date
Application number
PCT/IB2014/002141
Other languages
English (en)
French (fr)
Other versions
WO2014207573A3 (de
WO2014207573A2 (de
Inventor
Andreas Hilgeroth
Original Assignee
Martin-Luther-Universität Halle-Wittenberg
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 Martin-Luther-Universität Halle-Wittenberg filed Critical Martin-Luther-Universität Halle-Wittenberg
Priority to US14/900,366 priority Critical patent/US9901570B2/en
Priority to EP14799883.5A priority patent/EP3110421A2/de
Priority to JP2016522895A priority patent/JP2016530228A/ja
Publication of WO2014207573A2 publication Critical patent/WO2014207573A2/de
Publication of WO2014207573A8 publication Critical patent/WO2014207573A8/de
Publication of WO2014207573A3 publication Critical patent/WO2014207573A3/de

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
    • A61K31/435—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
    • A61K31/435—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
    • A61K31/4375—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 six-membered ring having nitrogen as a ring heteroatom, e.g. quinolizines, naphthyridines, berberine, vincamine
    • 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
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • 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

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Epidemiology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Abstract

2.1 Brustkrebs ist die nach epidemiologischen Daten häufigste Krebserkrankung bei Frauen. Besonders agressive Brustkrebserkrankungen sind durch ein invasives und Metastasen¬ bildendes Verhalten ausgezeichnet. Die Therapie solcher aggressiver Brustkrebserkrankungen ist äußerst problematisch und sehr kostspielig durch den Einsatz von spezifischen Antikörpern, die erst bei mehrfachen positiven histochemischen Testungen erfolgen. Aufgabe der Erfindung ist die Entwicklung neuer Enzyminhibitoren durch die Kombination in der Hemmung von Enzymen, die sowohl synergistisch als auch additiv das aggressive Brustzellwachstum bekämpfen. 2.2. Die erfindungsgemäß entwickelten pyridoannilierten Indole wirken selektiv hemmend auf die Enzyme HER2 und/oder Brk im nanomolaren bis picomolaren Konzentrationsbereich bei einem Screening an über 200 Kinasen des humanen Kinoms. Die er findungs gemäß entwickelten Enzyminhibitoren hemmen das Wachstum von Brustkrebszellen im nanomolaren Konzentrationsbereich ohne dabei kritische toxische Effekte zu zeigen. Die Derivatisierung in der 6-Position des 4-Chlor-a-Carbolins gelingt nebenproduktfrei und erfolgt ebenso wie die Derivatisierung in der Position 4 mit den Anilinderivaten in großer Reinheit mit quantitativen Ausbeuten. 2.3 Einsatz in der Medizin / Onkologie zur Therapie agressiver Brustkrebserkrankungen.
PCT/IB2014/002141 2013-06-26 2014-08-21 Brustkrebszellwachstum-hemmende enzyminhibitoren, verfahren zu ihrer herstellung sowie deren verwendung WO2014207573A2 (de)

Priority Applications (3)

Application Number Priority Date Filing Date Title
US14/900,366 US9901570B2 (en) 2013-06-26 2014-08-21 Breast cancer cell growth-inhibiting enzyme inhibitors, method for the production thereof, and use thereof
EP14799883.5A EP3110421A2 (de) 2013-06-26 2014-08-21 Brustkrebszellwachstum-hemmende enzyminhibitoren, verfahren zu ihrer herstellung sowie deren verwendung
JP2016522895A JP2016530228A (ja) 2013-06-26 2014-08-21 乳癌細胞の増殖を阻害する酵素阻害剤、その製造方法およびその使用

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
DE102013010603.6 2013-06-26
DE102013010603.6A DE102013010603A1 (de) 2013-06-26 2013-06-26 Brustkrebszellwachstum-hemmende Enzyminhibitoren, Verfahren zu ihrer Herstellung sowie deren Verwendung

Publications (3)

Publication Number Publication Date
WO2014207573A2 WO2014207573A2 (de) 2014-12-31
WO2014207573A8 true WO2014207573A8 (de) 2015-03-26
WO2014207573A3 WO2014207573A3 (de) 2015-05-14

Family

ID=51905309

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/IB2014/002141 WO2014207573A2 (de) 2013-06-26 2014-08-21 Brustkrebszellwachstum-hemmende enzyminhibitoren, verfahren zu ihrer herstellung sowie deren verwendung

Country Status (5)

Country Link
US (1) US9901570B2 (de)
EP (1) EP3110421A2 (de)
JP (1) JP2016530228A (de)
DE (1) DE102013010603A1 (de)
WO (1) WO2014207573A2 (de)

Families Citing this family (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US9890163B2 (en) 2015-10-15 2018-02-13 Princeton Drug Discovery Inc Inhibitors of protein kinases
US11773093B1 (en) * 2023-01-19 2023-10-03 King Faisal University N-(pyrimido[2,3-b]indol-7-yl)acetamide compounds as antibacterial agents

Family Cites Families (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2008542433A (ja) * 2005-06-09 2008-11-27 ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング ＣＤＫ−１インヒビターとしてのα−カルボリン
EP2161271A1 (de) * 2008-09-08 2010-03-10 Università Degli Studi Di Milano - Bicocca Alpha-Carbolin-Hemmer von NMP-ALK, RET und Bcr-Abl
EP2662372A1 (de) * 2012-05-11 2013-11-13 Università Degli Studi Di Milano - Bicocca Alpha-Carboline zur Behandlung von Krebs

Also Published As

Publication number Publication date
US9901570B2 (en) 2018-02-27
WO2014207573A3 (de) 2015-05-14
US20160235723A1 (en) 2016-08-18
JP2016530228A (ja) 2016-09-29
WO2014207573A2 (de) 2014-12-31
EP3110421A2 (de) 2017-01-04
DE102013010603A1 (de) 2014-12-31

Similar Documents

Publication Publication Date Title
UY36404A (es) ANTICUERPOS MONOCLONALES (Ab) COMO DETECTORES DE CD73 E INHIBIDORES DE SU ACTIVIDAD ENZIMÁTICA, Y COMPOSICIONES QUE LOS CONTIENEN
MX2015010124A (es) Mezclas de compuesto germinativo de espora deshidratada.
MX2019008428A (es) Inhibidores de glucosilceramida sintasa.
PH12015500431A1 (en) Glucosylceramide synthase inhibitors
MX2017006366A (es) Derivados de 6-amino-7-biciclo-7-deaza-purina como inhibidores de la proteina quinasa.
MX2012004210A (es) Derivados de pirazol como moduladores del canal de calcio activado por liberacion de calcio.
PH12014501439A1 (en) Plant artificial seeds having multilayers and methods for the production thereof
MX366130B (es) Inhibidores bivalentes de las proteinas iap y métodos terapéuticos que usan los mismos.
PH12014501407A1 (en) Plant artificial seeds and methods for the production thereof
MX2022008523A (es) Compuestos que interactuan con glicanos y metodos de uso.
MA34066B1 (fr) Composes de la pyrrolopyrimidine utilises en tant qu'inhibiteurs des cdk4/6
MX2017004128A (es) Derivados de diarilurea como inhibidores de quinasa p38.
EA201692483A1 (ru) Ингибиторы гистоновой метилазы
MX2015013945A (es) Derivados de urea utiles como inhibidores de quinasa.
MX342873B (es) Derivados de pirazolo-quinazolina sustituidos como inhibidores de cinasa.
WO2013025952A3 (en) Methods and compositions for the treatment and diagnosis of breast cancer
EA201790082A1 (ru) Ингибиторы лизин-специфической демитилазы-1
WO2014134084A3 (en) Phf20 and jmjd3 compositions and methods of use in cancer immunotherapy
CA2878796C (en) Derivatives of pyridinone as inhibitors for tissue transglutaminase
PH12017502112B1 (en) Pyrazole derivatives useful as 5-lipoxygenase activating protein (flap) inhibitors
MX2015012842A (es) Prodecimiento para preparar inhibidores de la glucosilceramida sintasa.
WO2014207573A8 (de) Brustkrebszellwachstum-hemmende enzyminhibitoren, verfahren zu ihrer herstellung sowie deren verwendung
WO2014130313A3 (en) Methods and compositions relating to the treatment of cancer
WO2016191703A3 (en) Tumor deliverable iron and protein synthesis inhibitors as a new class of drugs for the diagnosis and treatment of cancer
MX2020002730A (es) Metodos de preparacion de composiciones que contienen timoquinona.

Legal Events

Date Code Title Description
ENP Entry into the national phase in:

Ref document number: 2016522895

Country of ref document: JP

Kind code of ref document: A

REEP Request for entry into the european phase

Ref document number: 2014799883

Country of ref document: EP

WWE Wipo information: entry into national phase

Ref document number: 2014799883

Country of ref document: EP

WWE Wipo information: entry into national phase

Ref document number: 14900366

Country of ref document: US