RU99102852A - DERIVATIVES 11-ACETYL-12,13-DIOXABICYCLO [8.2.1] TRIDECENONE, METHOD FOR PRODUCING THEM AND CONTAINING THESE COMPOUNDS MEDICINES - Google Patents

DERIVATIVES 11-ACETYL-12,13-DIOXABICYCLO [8.2.1] TRIDECENONE, METHOD FOR PRODUCING THEM AND CONTAINING THESE COMPOUNDS MEDICINES

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Publication number
RU99102852A
RU99102852A RU99102852/04A RU99102852A RU99102852A RU 99102852 A RU99102852 A RU 99102852A RU 99102852/04 A RU99102852/04 A RU 99102852/04A RU 99102852 A RU99102852 A RU 99102852A RU 99102852 A RU99102852 A RU 99102852A
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RU
Russia
Prior art keywords
methyl
hydrogen
compound
acetyl
formula
Prior art date
Application number
RU99102852/04A
Other languages
Russian (ru)
Other versions
RU2218346C2 (en
Inventor
Даниель Жассеран
Ульф Пройшофф
Кристиан Эккхаут
Original Assignee
Солвей Фармасьютикалс Гмбх
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
Priority claimed from DE19805822A external-priority patent/DE19805822B4/en
Application filed by Солвей Фармасьютикалс Гмбх filed Critical Солвей Фармасьютикалс Гмбх
Publication of RU99102852A publication Critical patent/RU99102852A/en
Application granted granted Critical
Publication of RU2218346C2 publication Critical patent/RU2218346C2/en

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Claims (5)

1. Производные (2R,3S,4S,5R,6R,10R,11R)-2,4,6,8,10-пентаметил-11-ацетил-12,13-диоксабицикло[8.2.1]тридец-8-ен-1-она общей формулы I
Figure 00000001

где R1 обозначает водород или метил и
R2 обозначает водород или низший алканоил
и их физиологически приемлемые кислые аддитивные соли.
1. Derivatives (2R, 3S, 4S, 5R, 6R, 10R, 11R) -2,4,6,8,10-pentamethyl-11-acetyl-12,13-dioxabicyclo [8.2.1] tridets-8-ene -1-she of the general formula I
Figure 00000001

where R 1 denotes hydrogen or methyl and
R 2 is hydrogen or lower alkanoyl
and their physiologically acceptable acid addition salts.
2. Соединения по п. 1, где R1 обозначает метил.2. The compound of claim 1, wherein R 1 is methyl. 3. Соединения по п. 1 или 2, где R2 обозначает водород.3. The compound of claim 1 or 2, wherein R 2 is hydrogen. 4. Лекарственное средство, содержащее фармакологически эффективное количество соединения по п. 1 и обычные фармацевтические вспомогательные вещества и/или носители. 4. A medicament comprising a pharmacologically effective amount of a compound according to claim 1 and conventional pharmaceutical excipients and / or carriers. 5. Способ получения производных (2R,3S,4S,5R,6R,10R,11Р)-2,4,6,8,10-пентаметил-11-ацетил-12,13-диоксабицикло-[8.2.1] -тридец-8-ен-1-она общей формулы I,
Figure 00000002

где R1 обозначает водород или метил и
R2 обозначает водород или низший алканоил
и их физиологически приемлемых кислых аддитивных солей, отличающийся тем, что в соединении общей формулы II,
Figure 00000003

где R1 и R2 имеют вышеуказанные значения, 2',3'-дигидроксипент-2'-ильную боковую цепь в 11-положении циклической основной структуры переводят путем окислительного расщепления гликоля в боковую ацетильную цепь, и, в случае необходимости, в полученное соединение формулы I, где R1 обозначает водород, вводят метильный остаток R1 или в полученном соединении формулы I, где R1 обозначает метил, отщепляют метильный остаток R1, и, в случае необходимости, свободные соединения формулы I переводят в их стабильные кислые аддитивные соли или кислые аддитивные соли переводят в свободные соединения формулы I.
5. A method of obtaining derivatives of (2R, 3S, 4S, 5R, 6R, 10R, 11P) -2,4,6,8,10-pentamethyl-11-acetyl-12,13-dioxabicyclo- [8.2.1] -tride -8-en-1-one of general formula I,
Figure 00000002

where R 1 denotes hydrogen or methyl and
R 2 is hydrogen or lower alkanoyl
and their physiologically acceptable acid addition salts, characterized in that in the compound of General formula II,
Figure 00000003

where R 1 and R 2 have the above meanings, the 2 ′, 3′-dihydroxypent-2′-yl side chain at the 11-position of the cyclic main structure is converted by oxidative cleavage of the glycol to the side acetyl chain, and, if necessary, to the obtained compound of the formula I, where R 1 is hydrogen, a methyl residue R 1 is introduced, or in the resulting compound of the formula I, where R 1 is methyl, the methyl residue R 1 is cleaved and, if necessary, the free compounds of the formula I are converted into their stable acid addition salts or acidic additive oli converted into the free compounds of formula I.
RU99102852/04A 1998-02-13 1999-02-12 Derivatives of 11-acetyl-12,13-dioxabicyclo[8,2,1]- tridecenone, method for their preparing and medicinal agent comprising these compounds RU2218346C2 (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
DE19805822.5 1998-02-13
DE19805822A DE19805822B4 (en) 1998-02-13 1998-02-13 11-Acetyl-12,13-dioxabicyclo [8.2.1] tridecenone derivatives, process for their preparation and medicaments containing these compounds

Publications (2)

Publication Number Publication Date
RU99102852A true RU99102852A (en) 2000-12-20
RU2218346C2 RU2218346C2 (en) 2003-12-10

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Country Status (26)

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EP (1) EP0937734B1 (en)
JP (1) JPH11269193A (en)
KR (1) KR100584017B1 (en)
CN (1) CN1189473C (en)
AR (1) AR014320A1 (en)
AT (1) ATE486083T1 (en)
AU (1) AU748670B2 (en)
BR (1) BR9900442A (en)
CA (1) CA2260315C (en)
CZ (1) CZ294879B6 (en)
DE (2) DE19805822B4 (en)
DZ (1) DZ2721A1 (en)
ES (1) ES2355187T3 (en)
HK (1) HK1023575A1 (en)
HU (1) HU222539B1 (en)
ID (1) ID21968A (en)
IL (1) IL128238A (en)
NO (1) NO310917B1 (en)
NZ (1) NZ334087A (en)
PL (1) PL192281B1 (en)
RU (1) RU2218346C2 (en)
SK (1) SK285313B6 (en)
TR (1) TR199900285A3 (en)
TW (1) TW579379B (en)
UA (1) UA57030C2 (en)
ZA (1) ZA99678B (en)

Families Citing this family (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE60027015T2 (en) * 2000-08-17 2006-10-05 The Kitasato Institute Pseudoerythromycin DERIVATIVES
GB0611907D0 (en) 2006-06-15 2006-07-26 Glaxo Group Ltd Compounds
JP2009501199A (en) 2005-07-12 2009-01-15 グラクソ グループ リミテッド Piperazine heteroaryl derivatives as GPR38 agonists
NZ565062A (en) 2005-07-26 2011-02-25 Glaxo Group Ltd Benzylpiperazine derivates and their use in treating conditions mediated by GPR38 receptors
ES2344484T3 (en) 2006-06-28 2010-08-27 Glaxo Group Limited PIPERAZINYL DERIVATIVES USEFUL IN THE TREATMENT OF DISEASES MEDIATED BY THE GPR38 RECEIVER
CA2750699C (en) 2009-02-27 2015-12-29 Raqualia Pharma Inc. Oxyindole derivatives with motilin receptor agonistic activity

Family Cites Families (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5106961A (en) * 1987-05-26 1992-04-21 Eli Lilly And Company Erythromycin ring-contracted derivatives
US4920102A (en) * 1988-04-18 1990-04-24 Eli Lilly And Company Method for treating gastrointestinal disorders
NZ232375A (en) * 1989-02-09 1992-04-28 Lilly Co Eli Insulin analogues modified at b29
DE4200145A1 (en) * 1992-01-07 1993-07-08 Kali Chemie Pharma Gmbh 7,10-EPOXY-OXACYCLODODANE DERIVATIVES, METHODS AND INTERMEDIATE PRODUCTS FOR THEIR PREPARATION AND MEDICAMENTS CONTAINING THESE COMPOUNDS
US5712253A (en) * 1996-06-18 1998-01-27 Abbott Laboratories Macrocyclic 13-membered ring derivatives of erythromycins A and B

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