CR20160432A - Inhibidores de las vías de señalización de wnt - Google Patents

Inhibidores de las vías de señalización de wnt

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Publication number
CR20160432A
CR20160432A CR20160432A CR20160432A CR20160432A CR 20160432 A CR20160432 A CR 20160432A CR 20160432 A CR20160432 A CR 20160432A CR 20160432 A CR20160432 A CR 20160432A CR 20160432 A CR20160432 A CR 20160432A
Authority
CR
Costa Rica
Prior art keywords
compounds
inhibitors
wnt signaling
preparing
signaling road
Prior art date
Application number
CR20160432A
Other languages
English (en)
Inventor
Stefan Golz
Dirk; Schneider
Manfred Möwes
Jens; Geisler
Eckhard Bender
Franziska Siegel
Ludwig Zorn
Florian Puehler
Andrea Hägebarth
Philip Lienau
Daniel Basting
Anja Giese
Kai Thede
Ursula Mönning
Ningshu Liu
William J Scott
Original Assignee
Bayer Pharma AG
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 Bayer Pharma AG filed Critical Bayer Pharma AG
Publication of CR20160432A publication Critical patent/CR20160432A/es

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    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
    • C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
    • C07D491/08—Bridged systems
    • 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
    • C07D401/14—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 three or more hetero rings
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    • 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
    • A61K31/4965—Non-condensed pyrazines
    • A61K31/497—Non-condensed pyrazines containing further heterocyclic rings
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    • 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
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    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
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    • A61K31/53—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with three nitrogens as the only ring hetero atoms, e.g. chlorazanil, melamine
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    • A61K31/54—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 sulfur as the ring hetero atoms, e.g. sulthiame
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    • A61K9/2004—Excipients; Inactive ingredients
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    • A61K9/205—Polysaccharides, e.g. alginate, gums; Cyclodextrin
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    • A61K9/48—Preparations in capsules, e.g. of gelatin, of chocolate
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    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C205/00—Compounds containing nitro groups bound to a carbon skeleton
    • C07C205/45—Compounds containing nitro groups bound to a carbon skeleton the carbon skeleton being further substituted by at least one doubly—bound oxygen atom, not being part of a —CHO group
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    • C07C205/59—Compounds containing nitro groups bound to a carbon skeleton the carbon skeleton being further substituted by carboxyl groups having nitro groups and carboxyl groups bound to carbon atoms of six-membered aromatic rings of the carbon skeleton the carbon skeleton being further substituted by singly-bound oxygen atoms
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    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C229/00—Compounds containing amino and carboxyl groups bound to the same carbon skeleton
    • C07C229/52—Compounds containing amino and carboxyl groups bound to the same carbon skeleton having amino and carboxyl groups bound to carbon atoms of six-membered aromatic rings of the same carbon skeleton
    • C07C229/54—Compounds containing amino and carboxyl groups bound to the same carbon skeleton having amino and carboxyl groups bound to carbon atoms of six-membered aromatic rings of the same carbon skeleton with amino and carboxyl groups bound to carbon atoms of the same non-condensed six-membered aromatic ring
    • C07C229/64—Compounds containing amino and carboxyl groups bound to the same carbon skeleton having amino and carboxyl groups bound to carbon atoms of six-membered aromatic rings of the same carbon skeleton with amino and carboxyl groups bound to carbon atoms of the same non-condensed six-membered aromatic ring the carbon skeleton being further substituted by singly-bound oxygen atoms
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    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C233/00—Carboxylic acid amides
    • C07C233/01—Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms
    • C07C233/16—Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by singly-bound oxygen atoms
    • C07C233/24—Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by singly-bound oxygen atoms with the substituted hydrocarbon radical bound to the nitrogen atom of the carboxamide group by a carbon atom of a six-membered aromatic ring
    • C07C233/25—Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by singly-bound oxygen atoms with the substituted hydrocarbon radical bound to the nitrogen atom of the carboxamide group by a carbon atom of a six-membered aromatic ring having the carbon atom of the carboxamide group bound to a hydrogen atom or to a carbon atom of an acyclic saturated carbon skeleton
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    • C07C233/00—Carboxylic acid amides
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    • C07C233/53—Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by carboxyl groups with the substituted hydrocarbon radical bound to the nitrogen atom of the carboxamide group by a carbon atom of a six-membered aromatic ring
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    • 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
    • C07D295/14—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 carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C07D295/145—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 carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals with the ring nitrogen atoms and the carbon atoms with three bonds to hetero atoms attached to the same carbon chain, which is not interrupted by carbocyclic rings
    • C07D295/15—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 carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals with the ring nitrogen atoms and the carbon atoms with three bonds to hetero atoms attached to the same carbon chain, which is not interrupted by carbocyclic rings to an acyclic saturated chain
    • 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
    • C07D401/04—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 directly linked by a ring-member-to-ring-member bond
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    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing three or more hetero rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K2300/00—Mixtures or combinations of active ingredients, wherein at least one active ingredient is fully defined in groups A61K31/00 - A61K41/00
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    • A61K9/0007—Effervescent
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    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/0012—Galenical forms characterised by the site of application
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    • A61K9/0056—Mouth soluble or dispersible forms; Suckable, eatable, chewable coherent forms; Forms rapidly disintegrating in the mouth; Lozenges; Lollipops; Bite capsules; Baked products; Baits or other oral forms for animals
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    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/20—Pills, tablets, discs, rods
    • A61K9/2004—Excipients; Inactive ingredients
    • A61K9/2013—Organic compounds, e.g. phospholipids, fats
    • A61K9/2018—Sugars, or sugar alcohols, e.g. lactose, mannitol; Derivatives thereof, e.g. polysorbates
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    • A61K9/2004—Excipients; Inactive ingredients
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    • A61K9/2004—Excipients; Inactive ingredients
    • A61K9/2022—Organic macromolecular compounds
    • A61K9/2063—Proteins, e.g. gelatin

Abstract

La presente invención se refiere a inhibidores de las vías de señalización de Wnt de la fórmula general (I) como se describe y se define en la presente, a métodos de preparación de dichos compuestos, a compuestos intermediarios útiles para preparar dichos compuestos, a composiciones farmacéuticas y combinaciones que comprenden dichos compuestos y al uso de dichos compuestos para producir una composición farmacéutica para el tratamiento o la prevención de una enfermedad, en particular de un trastorno hiperproliferativo, como un único agente o en combinación con otros ingredientes activos
CR20160432A 2014-03-20 2015-03-18 Inhibidores de las vías de señalización de wnt CR20160432A (es)

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US201461968175P 2014-03-20 2014-03-20
PCT/EP2015/055631 WO2015140196A1 (en) 2014-03-20 2015-03-18 Inhibitors of the wnt signalling pathways

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DO (1) DOP2016000251A (es)
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EA201500953A1 (ru) 2013-03-20 2016-06-30 Байер Фарма Акциенгезельшафт 3-ацетиламино-1-(фенилгетероариламинокарбонил или фенилгетероарилкарбониламино)бензольные производные для лечения гиперпролиферативных нарушений
BR112016021626A2 (pt) 2014-03-20 2018-05-15 Samumed, Llc indazol-3-carboxamidas 5-substituídas e preparação e uso das mesmas
WO2017167150A1 (zh) * 2016-03-31 2017-10-05 苏州云轩医药科技有限公司 一种3-氟吡啶杂环化合物及其应用
CN109879818A (zh) * 2019-04-04 2019-06-14 安徽丰乐农化有限责任公司 N-(4,6-二甲氧基嘧啶-2-基)-4-甲砜基-2-硝基苯甲酰胺的合成方法
CN115850202A (zh) * 2022-12-26 2023-03-28 上海科技大学 一种卷曲受体7的小分子抑制剂及其制备方法和应用

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WO2000007991A1 (en) * 1998-08-04 2000-02-17 Astrazeneca Ab Amide derivatives useful as inhibitors of the production of cytokines
WO2000055120A1 (en) * 1999-03-17 2000-09-21 Astrazeneca Ab Amide derivatives
CN1950332A (zh) * 2004-03-02 2007-04-18 神经能质公司 经杂烷基取代的联苯－4－羧酸芳基醯胺类似物
US7776869B2 (en) * 2004-10-18 2010-08-17 Amgen Inc. Heteroaryl-substituted alkyne compounds and method of use
DE602006021591D1 (de) * 2006-12-11 2011-06-09 Genetics Co Inc Aromatische 1,4-DI-Carboxylamide und deren Verwendung
WO2013093508A2 (en) * 2011-12-22 2013-06-27 Oslo University Hospital Hf Wnt pathway inhibitors
CN105579457B (zh) * 2013-03-20 2017-08-04 拜耳制药股份公司 取代的n‑联苯‑3‑乙酰基氨基‑苯甲酰胺和n‑[3‑(乙酰基氨基)苯基]‑联苯‑甲酰胺及其作为wnt信号通路抑制剂用途
EA201500953A1 (ru) * 2013-03-20 2016-06-30 Байер Фарма Акциенгезельшафт 3-ацетиламино-1-(фенилгетероариламинокарбонил или фенилгетероарилкарбониламино)бензольные производные для лечения гиперпролиферативных нарушений
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CL2016002354A1 (es) 2017-03-10
JP2017511309A (ja) 2017-04-20
CU20160139A7 (es) 2017-04-05
US20170114070A1 (en) 2017-04-27
DOP2016000251A (es) 2016-10-31
WO2015140196A1 (en) 2015-09-24
CN106459072A (zh) 2017-02-22
AU2015233559A1 (en) 2016-09-15
EA201691878A1 (ru) 2017-12-29
AP2016009433A0 (en) 2016-09-30
CA2943001A1 (en) 2015-09-24
BR112016021656A2 (pt) 2017-10-24
SG11201606913PA (en) 2016-10-28
MX2016012173A (es) 2017-01-19
IL247366A0 (en) 2016-11-30
PH12016501814A1 (en) 2016-11-07
KR20160127838A (ko) 2016-11-04
PE20170187A1 (es) 2017-04-01
EP3119787A1 (en) 2017-01-25

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