EA201490642A1 - Производные анилина, их получение и терапевтическое применение - Google Patents

Производные анилина, их получение и терапевтическое применение

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Publication number
EA201490642A1
EA201490642A1 EA201490642A EA201490642A EA201490642A1 EA 201490642 A1 EA201490642 A1 EA 201490642A1 EA 201490642 A EA201490642 A EA 201490642A EA 201490642 A EA201490642 A EA 201490642A EA 201490642 A1 EA201490642 A1 EA 201490642A1
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EA
Eurasian Patent Office
Prior art keywords
alkyl
obtaining
aniline derivatives
therapeutic application
halogen
Prior art date
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EA201490642A
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English (en)
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EA026702B1 (ru
Inventor
Джон Фьютрилл
Каролин Лериш
Дэвид Мидлмисс
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Фовеа Фармасьютикалз
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Priority claimed from EP20110306170 external-priority patent/EP2570402A1/en
Priority claimed from EP12305130.2A external-priority patent/EP2623490A1/en
Application filed by Фовеа Фармасьютикалз filed Critical Фовеа Фармасьютикалз
Publication of EA201490642A1 publication Critical patent/EA201490642A1/ru
Publication of EA026702B1 publication Critical patent/EA026702B1/ru

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    • C07C217/78—Compounds containing amino and etherified hydroxy groups bound to the same carbon skeleton having amino groups and etherified hydroxy groups bound to carbon atoms of six-membered aromatic rings of the same carbon skeleton
    • C07C217/80—Compounds containing amino and etherified hydroxy groups bound to the same carbon skeleton having amino groups and etherified hydroxy groups bound to carbon atoms of six-membered aromatic rings of the same carbon skeleton having amino groups and etherified hydroxy groups bound to carbon atoms of non-condensed six-membered aromatic rings
    • C07C217/82—Compounds containing amino and etherified hydroxy groups bound to the same carbon skeleton having amino groups and etherified hydroxy groups bound to carbon atoms of six-membered aromatic rings of the same carbon skeleton having amino groups and etherified hydroxy groups bound to carbon atoms of non-condensed six-membered aromatic rings of the same non-condensed six-membered aromatic ring
    • C07C217/84—Compounds containing amino and etherified hydroxy groups bound to the same carbon skeleton having amino groups and etherified hydroxy groups bound to carbon atoms of six-membered aromatic rings of the same carbon skeleton having amino groups and etherified hydroxy groups bound to carbon atoms of non-condensed six-membered aromatic rings of the same non-condensed six-membered aromatic ring the oxygen atom of at least one of the etherified hydroxy groups being further bound to an acyclic carbon atom
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    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/16—Amides, e.g. hydroxamic acids
    • A61K31/165—Amides, e.g. hydroxamic acids having aromatic rings, e.g. colchicine, atenolol, progabide
    • 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
    • A61K31/196—Carboxylic acids, e.g. valproic acid having an amino group the amino group being directly attached to a ring, e.g. anthranilic acid, mefenamic acid, diclofenac, chlorambucil
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    • A61K31/21—Esters, e.g. nitroglycerine, selenocyanates
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    • 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
    • A61K31/535—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 oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/5375—1,4-Oxazines, e.g. morpholine
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    • C07C213/08—Preparation of compounds containing amino and hydroxy, amino and etherified hydroxy or amino and esterified hydroxy groups bound to the same carbon skeleton by reactions not involving the formation of amino groups, hydroxy groups or etherified or esterified hydroxy groups
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    • C07C233/75—Carboxylic acid amides having carbon atoms of carboxamide groups bound to carbon atoms of six-membered aromatic rings 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
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    • C07C235/02—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms having carbon atoms of carboxamide groups bound to acyclic carbon atoms and singly-bound oxygen atoms bound to the same carbon skeleton
    • C07C235/04—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms having carbon atoms of carboxamide groups bound to acyclic carbon atoms and singly-bound oxygen atoms bound to the same carbon skeleton the carbon skeleton being acyclic and saturated
    • C07C235/18—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms having carbon atoms of carboxamide groups bound to acyclic carbon atoms and singly-bound oxygen atoms bound to the same carbon skeleton the carbon skeleton being acyclic and saturated having at least one of the singly-bound oxygen atoms further bound to a carbon atom of a six-membered aromatic ring, e.g. phenoxyacetamides
    • C07C235/20—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms having carbon atoms of carboxamide groups bound to acyclic carbon atoms and singly-bound oxygen atoms bound to the same carbon skeleton the carbon skeleton being acyclic and saturated having at least one of the singly-bound oxygen atoms further bound to a carbon atom of a six-membered aromatic ring, e.g. phenoxyacetamides having the nitrogen atoms of the carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms
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    • 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
    • C07C235/56—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 having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a six-membered aromatic ring
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    • C07C237/28—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups having the carbon atom of at least one of the carboxamide groups bound to a carbon atom of a non-condensed six-membered aromatic ring of the carbon skeleton
    • C07C237/30—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups having the carbon atom of at least one of the carboxamide groups bound to a carbon atom of a non-condensed six-membered aromatic ring of the carbon skeleton having the nitrogen atom of the carboxamide group bound to hydrogen atoms or to acyclic carbon atoms
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    • C07D295/084—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 singly bound oxygen or sulfur atoms with the ring nitrogen atoms and the oxygen or sulfur atoms attached to the same carbon chain, which is not interrupted by carbocyclic rings
    • C07D295/088—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 singly bound oxygen or sulfur atoms with the ring nitrogen atoms and the oxygen or sulfur atoms attached to the same carbon chain, which is not interrupted by carbocyclic rings to an acyclic saturated chain

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
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  • Epidemiology (AREA)
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  • Ophthalmology & Optometry (AREA)
  • Emergency Medicine (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Dermatology (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)

Abstract

Изобретение касается производных анилина формулы (I), их получения и терапевтического применения, например, для лечения глаукомы: в формуле (I) R1a обозначает Н, галоген, (C-C)алкил или CN; R1b обозначает Н, галоген или (C-C)алкил; R1c обозначает Н или (C-C)алкил; R2 обозначает Н, галоген, ОН, O-(C-C)алкил или (C-C)алкил; R3 обозначает Н, галоген, (C-C)алкил, ОН, О-(C-C)алкил, CONHили CN; R4 обозначает Н, галоген или (C-C)алкил; R5 обозначает Н или F; R7 обозначает Н или F; R8 обозначает Н или F; R9 обозначает Н или (C-C)алкил; или одного из их энантиомеров.
EA201490642A 2011-09-16 2012-09-07 Производные анилина, их получение и терапевтическое применение EA026702B1 (ru)

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
EP20110306170 EP2570402A1 (en) 2011-09-16 2011-09-16 Bi-aryl derivatives, their preparation and their therapeutic application
EP12305130.2A EP2623490A1 (en) 2012-02-03 2012-02-03 2-(3-aminophenoxy)-acetic acid derivatives as EP2 receptor agonists for use in treatment of glaucoma
EP12305626 2012-06-04
PCT/EP2012/067473 WO2013037705A2 (en) 2011-09-16 2012-09-07 Aniline derivatives,their preparation and their therapeutic application

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EA201490642A1 true EA201490642A1 (ru) 2014-07-30
EA026702B1 EA026702B1 (ru) 2017-05-31

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US (2) US9249085B2 (ru)
EP (1) EP2755944B1 (ru)
JP (2) JP2014530177A (ru)
KR (1) KR20140097127A (ru)
CN (1) CN103930396B (ru)
AR (1) AR087814A1 (ru)
AU (1) AU2012307527B2 (ru)
BR (1) BR112014005935A2 (ru)
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CO (1) CO6910193A2 (ru)
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EC (1) ECSP14013249A (ru)
GT (1) GT201400050A (ru)
IL (1) IL231444A (ru)
MA (1) MA35816B1 (ru)
MX (1) MX347855B (ru)
NI (1) NI201400021A (ru)
PE (1) PE20142083A1 (ru)
SG (1) SG11201400555SA (ru)
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WO2016001452A1 (en) 2014-07-04 2016-01-07 Universität Zürich Compounds, in particular for use in the treatment of a disease or condition for which a bromodomain inhibitor is indicated
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CN106905181B (zh) * 2017-04-14 2018-10-09 上海海洋大学 一种立达霉代谢产物16的合成方法
CN107162921B (zh) * 2017-05-27 2019-12-13 中国药科大学 一类苯氧乙酸衍生物、其制备方法及其作为药物的用途
CN112920078A (zh) * 2019-12-05 2021-06-08 武汉珈汇精化科技有限公司 一种制备4-氰基苯甲酸甲酯的方法和一种制备4-氰基苯甲酸的方法
CN113651715B (zh) * 2021-09-13 2023-12-08 江苏弘和药物研发有限公司 一种一锅法合成香豆酰多巴胺的方法
CN113636949A (zh) * 2021-09-13 2021-11-12 江苏弘和药物研发有限公司 一种一锅法合成咖啡酰多巴胺的方法

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JP6272976B2 (ja) 2018-01-31
CO6910193A2 (es) 2014-03-31
NZ622329A (en) 2015-05-29
CA2848229C (en) 2019-08-27
CN103930396A (zh) 2014-07-16
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