BRPI1014174B8 - uso de um composto selecionado a partir de 4-((1s)-1-{[5-cloro-2-(4-fluorofenóxi)benzoil]amino}etil)ácido benzóico, 4-[(1s)-1-({[5-cloro-2-(3-fluorofenóxi)piridin-3-il]carbonil}amino)etil]ácido benzóico e 3-[2-(4-{2-etil-4,6-dimetil-1h-imidazo[4,5-c]piridin-1-il}fenil)etil]-1-[(4-metilbenzeno)sulfonil]urea para tratamento de um câncer epitelial relacionado à pge2 - Google Patents

uso de um composto selecionado a partir de 4-((1s)-1-{[5-cloro-2-(4-fluorofenóxi)benzoil]amino}etil)ácido benzóico, 4-[(1s)-1-({[5-cloro-2-(3-fluorofenóxi)piridin-3-il]carbonil}amino)etil]ácido benzóico e 3-[2-(4-{2-etil-4,6-dimetil-1h-imidazo[4,5-c]piridin-1-il}fenil)etil]-1-[(4-metilbenzeno)sulfonil]urea para tratamento de um câncer epitelial relacionado à pge2

Info

Publication number
BRPI1014174B8
BRPI1014174B8 BRPI1014174A BRPI1014174A BRPI1014174B8 BR PI1014174 B8 BRPI1014174 B8 BR PI1014174B8 BR PI1014174 A BRPI1014174 A BR PI1014174A BR PI1014174 A BRPI1014174 A BR PI1014174A BR PI1014174 B8 BRPI1014174 B8 BR PI1014174B8
Authority
BR
Brazil
Prior art keywords
ethyl
fluorophenoxy
pyridin
chloro
amino
Prior art date
Application number
BRPI1014174A
Other languages
English (en)
Inventor
Nonomura Kazuhiko
Koizumi Shinichi
Okumura Takako
Take Yukinori
Original Assignee
Askat Inc
Raqualia Pharma Inc
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 Askat Inc, Raqualia Pharma Inc filed Critical Askat Inc
Publication of BRPI1014174A2 publication Critical patent/BRPI1014174A2/pt
Publication of BRPI1014174B1 publication Critical patent/BRPI1014174B1/pt
Publication of BRPI1014174B8 publication Critical patent/BRPI1014174B8/pt

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
    • A61K31/185—Acids; Anhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic or hydroximic acids
    • A61K31/19—Carboxylic acids, e.g. valproic acid
    • A61K31/192—Carboxylic acids, e.g. valproic acid having aromatic groups, e.g. sulindac, 2-aryl-propionic acids, ethacrynic acid 
    • 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
    • A61K31/185—Acids; Anhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic or hydroximic acids
    • A61K31/19—Carboxylic acids, e.g. valproic acid
    • A61K31/195—Carboxylic acids, e.g. valproic acid having an amino group
    • 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
    • A61K31/275—Nitriles; Isonitriles
    • A61K31/277—Nitriles; Isonitriles having a ring, e.g. verapamil
    • 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
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/4164—1,3-Diazoles
    • A61K31/4184—1,3-Diazoles condensed with carbocyclic rings, e.g. benzimidazoles
    • 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
    • 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
    • A61K31/4412—Non condensed pyridines; Hydrogenated derivatives thereof having oxo groups directly attached to the heterocyclic ring
    • 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
    • A61K31/4439—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
    • 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
    • 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
    • A61P35/04—Antineoplastic agents specific for metastasis
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C235/00—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms
    • C07C235/42—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms having carbon atoms of carboxamide groups bound to carbon atoms of six-membered aromatic rings and singly-bound oxygen atoms bound to the same carbon skeleton
    • C07C235/44—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms having carbon atoms of carboxamide groups bound to carbon atoms of six-membered aromatic rings and singly-bound oxygen atoms bound to the same carbon skeleton with carbon atoms of carboxamide groups and singly-bound oxygen atoms bound to carbon atoms of the same non-condensed six-membered aromatic ring
    • C07C235/58—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms having carbon atoms of carboxamide groups bound to carbon atoms of six-membered aromatic rings and singly-bound oxygen atoms bound to the same carbon skeleton with carbon atoms of carboxamide groups and singly-bound oxygen atoms bound to carbon atoms of the same non-condensed six-membered aromatic ring with carbon atoms of carboxamide groups and singly-bound oxygen atoms, bound in ortho-position to carbon atoms of the same non-condensed six-membered aromatic ring
    • C07C235/60—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms having carbon atoms of carboxamide groups bound to carbon atoms of six-membered aromatic rings and singly-bound oxygen atoms bound to the same carbon skeleton with carbon atoms of carboxamide groups and singly-bound oxygen atoms bound to carbon atoms of the same non-condensed six-membered aromatic ring with carbon atoms of carboxamide groups and singly-bound oxygen atoms, bound in ortho-position to carbon atoms of the same non-condensed six-membered aromatic ring having the nitrogen atoms of the carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D213/78—Carbon atoms having three bonds to hetero atoms, with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C07D213/81—Amides; Imides
    • C07D213/82—Amides; Imides in position 3
    • 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
    • A61K2121/00—Preparations for use in therapy

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Organic Chemistry (AREA)
  • Epidemiology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Oncology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Pyridine Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)

Abstract

uso de um composto da formula (i), (ii) (ill) ou (iv) ou um sal farmaceuticamente aceitável seu para a fabricação de um medicamento para o tratamento de câncer em um humano ou um animal; método para o tratamento de câncer, pacote comercial,método para redução de células cancerosas e kit para o tratamento de câncer. esta invenção prove um medicamento para o tratamento do câncer, que provoca a redução do câncer. esta invenção refere-se ao uso de um composto que tem atividade inibidoras contra o receptor de prostaglandina e2 (receptor de ep4) e é representado pela seguinte formula geral (i), (il), (ill) ou (iv) ou um sal farmaceuticamente aceitável seu, ou uma composição farmacêutica compreendendo composto ou o sal para a fabricação de um medicamento para o tratamento de câncer. a invenção refere-se a um método para tratamento do câncer compreendendo administrar o composto ou um sal farmaceuticamente aceitável seu, ou uma composição farmacêutica compreendendo o composto ou o sal aos humanos ou animais.o composto ou um sal farmaceuticamente aceitável seu, ou a composição farmacêutica pode ser usado em combinação com um ou mais segundos agentes ativos.
BRPI1014174A 2009-04-22 2010-04-22 uso de um composto selecionado a partir de 4-((1s)-1-{[5-cloro-2-(4-fluorofenóxi)benzoil]amino}etil)ácido benzóico, 4-[(1s)-1-({[5-cloro-2-(3-fluorofenóxi)piridin-3-il]carbonil}amino)etil]ácido benzóico e 3-[2-(4-{2-etil-4,6-dimetil-1h-imidazo[4,5-c]piridin-1-il}fenil)etil]-1-[(4-metilbenzeno)sulfonil]urea para tratamento de um câncer epitelial relacionado à pge2 BRPI1014174B8 (pt)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
JP2009104568 2009-04-22
JP2009104568 2009-04-22
JP2010015445 2010-01-27
JP2010015445 2010-01-27
PCT/JP2010/057114 WO2010123049A1 (ja) 2009-04-22 2010-04-22 癌治療のための選択的ep4受容体拮抗物質

Publications (3)

Publication Number Publication Date
BRPI1014174A2 BRPI1014174A2 (pt) 2016-04-05
BRPI1014174B1 BRPI1014174B1 (pt) 2020-10-06
BRPI1014174B8 true BRPI1014174B8 (pt) 2021-05-25

Family

ID=43011165

Family Applications (1)

Application Number Title Priority Date Filing Date
BRPI1014174A BRPI1014174B8 (pt) 2009-04-22 2010-04-22 uso de um composto selecionado a partir de 4-((1s)-1-{[5-cloro-2-(4-fluorofenóxi)benzoil]amino}etil)ácido benzóico, 4-[(1s)-1-({[5-cloro-2-(3-fluorofenóxi)piridin-3-il]carbonil}amino)etil]ácido benzóico e 3-[2-(4-{2-etil-4,6-dimetil-1h-imidazo[4,5-c]piridin-1-il}fenil)etil]-1-[(4-metilbenzeno)sulfonil]urea para tratamento de um câncer epitelial relacionado à pge2

Country Status (11)

Country Link
US (5) US8921391B2 (pt)
EP (3) EP2965756B1 (pt)
JP (1) JP5668219B2 (pt)
KR (1) KR101575706B1 (pt)
CN (2) CN105596320B (pt)
BR (1) BRPI1014174B8 (pt)
CA (1) CA2754702C (pt)
ES (3) ES2698508T3 (pt)
MX (2) MX369117B (pt)
RU (1) RU2563817C2 (pt)
WO (1) WO2010123049A1 (pt)

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US10342785B2 (en) * 2016-11-04 2019-07-09 Askat Inc. Use of EP4 receptor antagonists for the treatment of NASH-associated liver cancer
CN107383004B (zh) * 2017-07-05 2020-04-17 浙江大学 2-氨基咪唑并吡啶类衍生物及制备和应用
CN112292128A (zh) * 2018-04-16 2021-01-29 阿瑞斯医疗有限公司 Ep4抑制剂和其用途
US20210315909A1 (en) 2018-07-11 2021-10-14 Arrys Therapeutics, Inc. Polymorphic compounds and uses thereof
IL280051B2 (en) * 2018-07-11 2024-03-01 Arrys Therapeutics Inc EP4 inhibitors and their synthesis
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GB201914585D0 (en) 2019-10-09 2019-11-20 Heptares Therapeutics Ltd Prostaglandin ep4 receptor antagonist compounds
WO2022247881A1 (zh) * 2021-05-28 2022-12-01 凯复(苏州)生物医药有限公司 治疗肿瘤的联合疗法
CN119634669B (zh) * 2024-11-12 2025-11-14 北京航空材料研究院股份有限公司 含有多角度管腔的蜡模制备方法
CN119657828B (zh) * 2024-11-12 2025-11-14 北京航空材料研究院股份有限公司 一种带多角度管腔型壳的制备方法及模具

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Also Published As

Publication number Publication date
EP2965756A1 (en) 2016-01-13
BRPI1014174B1 (pt) 2020-10-06
US9688674B2 (en) 2017-06-27
HK1214763A1 (en) 2016-08-05
JP5668219B2 (ja) 2015-02-12
MX2011011058A (es) 2011-11-18
ES2698508T3 (es) 2019-02-05
EP2422779A4 (en) 2013-06-19
MX369117B (es) 2019-10-28
KR20120096402A (ko) 2012-08-30
MX345032B (es) 2017-01-12
JPWO2010123049A1 (ja) 2012-10-25
US20120088723A1 (en) 2012-04-12
CN102421429A (zh) 2012-04-18
HK1166700A1 (en) 2012-11-09
US11840530B2 (en) 2023-12-12
US20170253595A1 (en) 2017-09-07
EP3431085A1 (en) 2019-01-23
US20150111920A1 (en) 2015-04-23
EP2422779B1 (en) 2016-01-06
WO2010123049A1 (ja) 2010-10-28
CN105596320B (zh) 2019-03-22
ES2960438T3 (es) 2024-03-04
US8921391B2 (en) 2014-12-30
RU2563817C2 (ru) 2015-09-20
US10611761B2 (en) 2020-04-07
CA2754702C (en) 2016-06-07
CA2754702A1 (en) 2010-10-28
US20200188367A1 (en) 2020-06-18
BRPI1014174A2 (pt) 2016-04-05
CN105596320A (zh) 2016-05-25
EP3431085C0 (en) 2023-10-11
ES2562814T3 (es) 2016-03-08
US10947235B2 (en) 2021-03-16
EP2422779A1 (en) 2012-02-29
EP3431085B1 (en) 2023-10-11
CN102421429B (zh) 2016-08-17
US20220073510A1 (en) 2022-03-10
KR101575706B1 (ko) 2015-12-10
EP2965756B1 (en) 2018-10-10

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