BR112016013618A8 - derivados de maleimida como moduladores de série de reação de wnt, seus usos, composição farmacêutica e processo para a preparação dos mesmos - Google Patents

derivados de maleimida como moduladores de série de reação de wnt, seus usos, composição farmacêutica e processo para a preparação dos mesmos Download PDF

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BR112016013618A8
BR112016013618A8 BR112016013618A BR112016013618A BR112016013618A8 BR 112016013618 A8 BR112016013618 A8 BR 112016013618A8 BR 112016013618 A BR112016013618 A BR 112016013618A BR 112016013618 A BR112016013618 A BR 112016013618A BR 112016013618 A8 BR112016013618 A8 BR 112016013618A8
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6alkyl
6alkoxy
optionally substituted
independently selected
substituents
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BR112016013618A
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BR112016013618A2 (pt
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Poulsen Anders
Jeyaraj Duraiswamy Athisayamani
Alam Jenefer
Yei Ho Soo
Ling Wang Wei
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Agency Science Tech & Res
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    • 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
    • A61K31/435—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
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/444—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring heteroatom, e.g. amrinone
    • 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
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    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
    • A—HUMAN NECESSITIES
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/18—Drugs for disorders of the alimentary tract or the digestive system for pancreatic disorders, e.g. pancreatic enzymes
    • A—HUMAN NECESSITIES
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    • A61P11/00—Drugs for disorders of the respiratory system
    • A—HUMAN NECESSITIES
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • A61P13/08—Drugs for disorders of the urinary system of the prostate
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • A61P13/10—Drugs for disorders of the urinary system of the bladder
    • A—HUMAN NECESSITIES
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    • A—HUMAN NECESSITIES
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    • A61P5/14—Drugs for disorders of the endocrine system of the thyroid hormones, e.g. T3, T4
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    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04—Ortho-condensed systems

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
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  • Physical Education & Sports Medicine (AREA)
  • Hematology (AREA)
  • Diabetes (AREA)
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  • Obesity (AREA)
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  • Pulmonology (AREA)
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  • Ophthalmology & Optometry (AREA)
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  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)

Abstract

a presente invenção se refere aos compostos de fórmula (i), combinações e usos dos mesmos para terapia de doença, ou um sal, solvato ou polimorfo farmaceuticamente aceitável do mesmo, incluindo todos os tautômeros e estereoisômeros, em que: r1 representa alquila opcionalmente substituída (em que substituintes opcionais incluem um ou mais substituintes cada qual independentemente selecionado de c1-6alcóxi); carbociclila opcionalmente substituída (em que substituintes opcionais incluem um ou mais substituintes cada qual independentemente selecionado de c1-6alquila, c1-6alcóxi, c1-6haloalquila, c1-6haloalcóxi e halo); ou ?alquilarila; r2 representa h; ou alquila; r3 representa h; ou alquila; u, v e w representam ?(ch2)-; ou u e v juntamente representam ?ch=ch- e w representa c=o; y representa arila; heteroarila; carbociclila opcionalmente substituída (em que substituintes opcionais incluem um ou mais substituintes cada qual independentemente selecionado de c1-6alquila, c1-6alcóxi, c1-6haloalquila, c1-6haloalcóxi e halo); ou heterociclila opcionalmente substituída (em que substituintes opcionais incluem um ou mais substituintes cada qual independentemente selecionado de c1-6alquila, c1-6alcóxi, -c(o)oc1-6alquila, -c(o)c1-6alquil e -c(o)nhc1-6alquil); e z representa arila; heteroarila; carbociclila opcionalmente substituída (em que substituintes opcionais incluem um ou mais substituintes cada qual independentemente selecionado de c1-6alquila, c1-6alcóxi, c1-6haloalquila, c1-6haloalcóxi e halo); ou heterociclila opcionalmente substituída (em que substituintes opcionais incluem um ou mais substituintes cada qual independentemente selecionado de c1-6alquila, c1-6alcóxi, -c(o)oc1-6alquila, -c(o)c1-6alquil e -c(o)nhc1-6alquil).
BR112016013618A 2013-12-17 2014-12-17 derivados de maleimida como moduladores de série de reação de wnt, seus usos, composição farmacêutica e processo para a preparação dos mesmos BR112016013618A8 (pt)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
GBGB1322334.2A GB201322334D0 (en) 2013-12-17 2013-12-17 Maleimide derivatives as modulators of WNT pathway
PCT/SG2014/000601 WO2015094118A1 (en) 2013-12-17 2014-12-17 Maleimide derivatives as modulators of wnt pathway

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BR112016013618A2 BR112016013618A2 (pt) 2017-08-08
BR112016013618A8 true BR112016013618A8 (pt) 2020-05-19

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US (1) US9981964B2 (pt)
EP (1) EP3083622B1 (pt)
JP (1) JP6511450B2 (pt)
KR (1) KR20160104010A (pt)
CN (1) CN106061974B (pt)
AU (1) AU2014367283B2 (pt)
BR (1) BR112016013618A8 (pt)
CA (1) CA2933682A1 (pt)
ES (1) ES2674096T3 (pt)
GB (1) GB201322334D0 (pt)
SG (1) SG11201604848UA (pt)
WO (1) WO2015094118A1 (pt)

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GB201322334D0 (en) 2013-12-17 2014-01-29 Agency Science Tech & Res Maleimide derivatives as modulators of WNT pathway
GB201409783D0 (en) * 2014-06-02 2014-07-16 Agency Science Tech & Res Phthalimide derivatives as modulators of WNT pathway
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CN109867661B (zh) * 2017-12-05 2022-07-19 中国医学科学院药物研究所 调节wnt信号通路的酰胺类化合物及其用途
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CN110317204B (zh) * 2019-08-02 2022-02-08 安徽农业大学 吡唑并嘧啶酮类衍生物及其制备方法和应用

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US9981964B2 (en) 2018-05-29
KR20160104010A (ko) 2016-09-02
AU2014367283B2 (en) 2018-05-24
US20160318926A1 (en) 2016-11-03
CN106061974B (zh) 2018-04-20
EP3083622B1 (en) 2018-03-21
ES2674096T3 (es) 2018-06-27
GB201322334D0 (en) 2014-01-29
AU2014367283A1 (en) 2016-06-23
SG11201604848UA (en) 2016-07-28
EP3083622A4 (en) 2017-05-10
BR112016013618A2 (pt) 2017-08-08
EP3083622A1 (en) 2016-10-26
JP2016540802A (ja) 2016-12-28
CN106061974A (zh) 2016-10-26
CA2933682A1 (en) 2015-06-25
WO2015094118A1 (en) 2015-06-25
JP6511450B2 (ja) 2019-05-15

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