SU509046A1 - Derivatives of 2-carbethoxy-3-aminoindole having antiinflammatory effect and process for preparing same - Google Patents

Derivatives of 2-carbethoxy-3-aminoindole having antiinflammatory effect and process for preparing same Download PDF

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Publication number
SU509046A1
SU509046A1 SU752106704A SU2106704A SU509046A1 SU 509046 A1 SU509046 A1 SU 509046A1 SU 752106704 A SU752106704 A SU 752106704A SU 2106704 A SU2106704 A SU 2106704A SU 509046 A1 SU509046 A1 SU 509046A1
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SU
USSR - Soviet Union
Prior art keywords
aminoindole
derivatives
carbethoxy
alkyl
hydrogen
Prior art date
Application number
SU752106704A
Other languages
Russian (ru)
Inventor
Г.Н. Курило
О.Н. Бояринцева
Е.А. Берлянд
С.С. Либерман
А.Н. Гринев
Original Assignee
Всесоюзный научно-исследовательский химико-фармацевтический институт им.Серго Орджоникидзе
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Priority to SU752106704A priority Critical patent/SU509046A1/en
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Publication of SU509046A1 publication Critical patent/SU509046A1/en

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Abstract

1. Производные 2-карбэтокси-З- -аминоиндола общей формулы I:где R' - водород, алкил, алкоксигруп-па, галоген; R - .водород, алкил,про вл ющие противовоспалительную активность.2. Способ получени  производных 2гкарбзтокси-3-аминоиндола,-о тли-' чающийс  тем, что соединени  общей формулы 1. Derivatives of 2-carbethoxy-3-α-aminoindole of the general formula I: where R 'is hydrogen, alkyl, alkoxygroup, halogen; R - hydrogen, alkyl, exhibiting anti-inflammatory activity. The method of obtaining the derivatives of 2g carbaztoxy-3-aminoindole, -o tly-, due to the fact that the compounds of the general formula

Description

Изобретение относитс  к новым химическим соединени м, а именно к производным 2-карбэтокси-З-аминоиндола общей формулы (1):The invention relates to new chemical compounds, namely, to derivatives of 2-carbethoxy-3-aminoindole of the general formula (1):

(I)(I)

COOCzHsCOOCzHs

гдеWhere

алкоксигруппа , галоген,alkoxy group, halogen,

Эти соединени  обладают выраженной противовоспалительной активностью, превосход щей активность противовоспалительного препарата бутадион.These compounds have a pronounced anti-inflammatory activity, superior to the activity of the anti-inflammatory drug butadione.

Противовоспалительное действие было изучено на нелинейных крысах при хроническом пролиферативном воспалении , вызванном введением под Ko-i жу живота инородных тел и при остром The anti-inflammatory effect was studied in non-linear rats in chronic proliferative inflammation caused by the introduction of foreign bodies under the Ko-i stomach and in acute

экссудативном воспалении, вызванном введением в плевральную или брюганую полость 0,25% раствора азотнокислого серебра.exudative inflammation caused by the introduction of a 0.25% solution of silver nitrate into the pleural or brutic cavity.

Все препараты вводили внутрь через зонд в желудок в виде водной взвеси в дозе 100 мг/кг. При лечении хронического воспалени  препарат вводили в день имплатации инородного тела и в последующие 6 дней. На 8-й день животных забивали.All drugs were injected through the probe into the stomach in the form of an aqueous suspension at a dose of 100 mg / kg. In the treatment of chronic inflammation, the drug was administered on the day of implantation of a foreign body and for the next 6 days. On the 8th day the animals were killed.

Показателем интенсивности воспалительного процесса  вл лс  вес образовавшихс  гранулем. При остром воспалении препараты вводили однократно за 30 мин до введени  азотнокислого серебра. Через 6 ч после введени  азотнокислого серебра животных забивали . Интенсивность воспалительного процесса определ ли по количеству экссудата в полости. Результаты приведены в таблице.An indicator of the intensity of the inflammatory process was the weight of the formed granulomas. For acute inflammation, the drugs were administered once 30 minutes before the introduction of silver nitrate. Six hours after the introduction of silver nitrate, the animals were killed. The intensity of the inflammatory process was determined by the amount of exudate in the cavity. The results are shown in the table.

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CMCM

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IT v.IT v.

COCO

oo

fcfc

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Claims (2)

1. Производные 2-карбэтокси-З-аминоиндола общей формулы I:1. Derivatives of 2-carbethoxy-3-aminoindole of the general formula I: ^TOl'TOOCjHs^ TOl'TOOCjHs R где R’ - водород, алкил, алкоксигруппа, галоген;R where R ’is hydrogen, alkyl, alkoxy, halogen; R -.водород, алкил, проявляющие противовоспалительную активность.R - hydrogen, alkyl, exhibiting anti-inflammatory activity. 2. Способ получения производных 2т-карбэтокси-3-аминоиндола,. о тличающийся тем, что соединения общей формулы (II):2. A method of obtaining derivatives of 2t-carbethoxy-3-aminoindole. o characterized in that the compounds of general formula (II): N=N-CfH5 соос2н5 (II), г реR и R1 имеют вышеуказанные значения, восстанавливают гидросульфитом натрия в спиртовой среде с последующим выделением целевого продукта·.·N = NC f H 5 coax 2 n 5 (II), g reR and R 1 have the above meanings, they are reduced with sodium hydrosulfite in an alcoholic medium, followed by isolation of the target product ·. · Изобретение относится к новым химическим соединениям, а именно к производным 2-карбэтокси-З-аминоиндола общей формулы (1):The invention relates to new chemical compounds, namely to derivatives of 2-carbethoxy-3-aminoindole of the general formula (1): ViT- ViT- t t ^СООС2Н5 (1) ^ SOOS 2 N 5 (1) R R где R - водород, where R is hydrogen, алкйл; alkyl; R*- водород, R * is hydrogen, алкйл, алкоксигруп· alkyl, alkoxygroup па, галоген. pa, halogen.
SU752106704A 1975-02-21 1975-02-21 Derivatives of 2-carbethoxy-3-aminoindole having antiinflammatory effect and process for preparing same SU509046A1 (en)

Priority Applications (1)

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SU752106704A SU509046A1 (en) 1975-02-21 1975-02-21 Derivatives of 2-carbethoxy-3-aminoindole having antiinflammatory effect and process for preparing same

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JP2008542291A (en) * 2005-05-26 2008-11-27 ニューロン システムズ Compositions and methods for treating retinal diseases
US9604997B2 (en) 2012-12-20 2017-03-28 Aldeyra Therapeutics, Inc. Peri-carbinols
US9687481B2 (en) 2013-01-23 2017-06-27 Aldeyra Therapeutics, Inc. Toxic aldehyde related diseases and treatment
US10111862B2 (en) 2013-01-25 2018-10-30 Aldeyra Therapeutics, Inc. Traps in the treatment of macular degeneration
US10414732B2 (en) 2017-03-16 2019-09-17 Aldeyra Therapeutics, Inc. Polymorphic compounds and uses thereof

Cited By (14)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US9650342B2 (en) 2005-05-26 2017-05-16 Aldeyra Therapeutics, Inc. Compositions and methods of treating retinal disease
JP2008542291A (en) * 2005-05-26 2008-11-27 ニューロン システムズ Compositions and methods for treating retinal diseases
US8940721B2 (en) 2005-05-26 2015-01-27 Aldexa Therapeutics, Inc. Compositions and methods of treating retinal disease
US9265759B2 (en) 2005-05-26 2016-02-23 Aldeyra Therapeutics, Inc. Compositions and methods of treating retinal disease
US9364471B2 (en) 2005-05-26 2016-06-14 Aldeyra Therapeutics, Inc. Compositions and methods of treating retinal disease
US10913722B2 (en) 2005-05-26 2021-02-09 Aldeyra Therapeutics, Inc. Compositions and methods of treating retinal disease
US8940764B2 (en) 2005-05-26 2015-01-27 Aldexa Therapeutics, Inc. Compositions and methods of treating retinal disease
US9896419B2 (en) 2005-05-26 2018-02-20 Aldeyra Therapeutics, Inc. Compositions and methods of treating retinal disease
US10202348B2 (en) 2005-05-26 2019-02-12 Aldeyra Therapeutics, Inc. Compositions and methods of treating retinal disease
US9604997B2 (en) 2012-12-20 2017-03-28 Aldeyra Therapeutics, Inc. Peri-carbinols
US9687481B2 (en) 2013-01-23 2017-06-27 Aldeyra Therapeutics, Inc. Toxic aldehyde related diseases and treatment
US10213395B2 (en) 2013-01-23 2019-02-26 Aldeyra Therapeutics, Inc. Toxic aldehyde related diseases and treatment
US10111862B2 (en) 2013-01-25 2018-10-30 Aldeyra Therapeutics, Inc. Traps in the treatment of macular degeneration
US10414732B2 (en) 2017-03-16 2019-09-17 Aldeyra Therapeutics, Inc. Polymorphic compounds and uses thereof

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