RU93058253A - COMPOUNDS-ANTIBIOTICS, METHODS FOR PRODUCING THEM, INTERMEDIATE COMPOUNDS, PHARMACEUTICAL COMPOSITION, METHOD OF TREATMENT - Google Patents

COMPOUNDS-ANTIBIOTICS, METHODS FOR PRODUCING THEM, INTERMEDIATE COMPOUNDS, PHARMACEUTICAL COMPOSITION, METHOD OF TREATMENT

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Publication number
RU93058253A
RU93058253A RU93058253/04A RU93058253A RU93058253A RU 93058253 A RU93058253 A RU 93058253A RU 93058253/04 A RU93058253/04 A RU 93058253/04A RU 93058253 A RU93058253 A RU 93058253A RU 93058253 A RU93058253 A RU 93058253A
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RU
Russia
Prior art keywords
group
alkyl
compounds
hydrogen
producing
Prior art date
Application number
RU93058253/04A
Other languages
Russian (ru)
Other versions
RU2117659C1 (en
Inventor
Джон Беттс Майкл
Морс Дэвис Гарет
Лингард Свейн Майкл
Original Assignee
Зенека Лимитед
Зенека-Фарма С.А.
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Priority claimed from GB929202298A external-priority patent/GB9202298D0/en
Application filed by Зенека Лимитед, Зенека-Фарма С.А. filed Critical Зенека Лимитед
Publication of RU93058253A publication Critical patent/RU93058253A/en
Application granted granted Critical
Publication of RU2117659C1 publication Critical patent/RU2117659C1/en

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Claims (1)

Изобретение относится к карбапенемам и обеспечивает соединение формулы
Figure 00000001

или его фармацевтически пригодную соль, или его эфир, гидролизируемый in vivo, где R1 - 1-оксиэтил, 1-фторэтил или оксиметил; R2 - водород или C1 - С4-алкил; R3 - водород или C1 - С4-алкил; R4 и R5 - одинаковые или разные и выбраны из водорода, галогена, цианогруппы, C1 - С4-алкила, нитрогруппы, гидроксила, карбоксила, C1 - С4-алкоксигруппы, C1 - С4- алкоксикарбонила, аминосульфонильной группы, C1 - С4- алкиламиносульфонильной группы, ди-C1 - С4- алкиламиносульфонильной группы, карбамоила, C1 - С4- алкилкарбамоила, ди-C1 - С4-алкилкарбамоила, трифторметила, сульфокислотной группы, аминогруппы, C1 - С4-алкиламиногруппы, ди-C1 - С4-алкиламиногруппы, C1 - С4-алканоиламиногруппы, C1 - С4-алканоил(N-C1 - С4- алкил)аминогруппы, C1 - С4-алкансульфонамидогруппы и C1 - С4-алкил S(O)n, где n = 0, 1 или 2; с условием, что в орто-положении к связи -NR3 - нет гидроксильного или карбоксильного заместителя. Способы получения таких соединений, промежуточные продукты при их получении, их применение в качестве терапевтических агентов и содержащие их фармацевтические композиции.The invention relates to carbapenems and provides a compound of the formula
Figure 00000001

or a pharmaceutically acceptable salt thereof, or an in vivo hydrolyzable ester thereof, wherein R 1 is 1-hydroxyethyl, 1-fluoroethyl or hydroxymethyl; R 2 is hydrogen or C 1 -C 4 alkyl; R 3 is hydrogen or C 1 -C 4 alkyl; R 4 and R 5 are the same or different and are selected from hydrogen, halogen, cyano group, C 1 - C 4 alkyl, nitro group, hydroxyl, carboxyl, C 1 - C 4 alkoxy group, C 1 - C 4 alkoxycarbonyl, aminosulfonyl group , C 1 - C 4 - alkylaminosulfonyl group, di-C 1 - C 4 - alkylaminosulfonyl group, carbamoyl, C 1 - C 4 - alkylcarbamoyl, di-C 1 - C 4 -alkylcarbamoyl, trifluoromethyl, sulfonic acid group, amino group, C 1 - C 4 alkylamino, di-C 1 - C 4 alkylamino, C 1 - C 4 alkanoylamino, C 1 - C 4 alkanoyl (NC 1 - C 4 - alkyl) amino, C 1 - C 4 alkanesulfonyl mido groups and C 1 -C 4 -alkyl S (O) n , where n = 0, 1 or 2; with the condition that in the ortho position to the —NR 3 bond there is no hydroxyl or carboxyl substituent. Methods for producing such compounds, intermediates in their preparation, their use as therapeutic agents and pharmaceutical compositions containing them.
RU93058253/04A 1992-02-04 1993-02-02 Carbopenem derivatives, their pharmaceutically acceptable salts and hydrolyzed in vivo esters (variants), method of synthesis (variants), pharmaceutical composition showing antibacterial activity, derivatives of pyrrolidine-4-ylthiol and protected derivatives of pyrrolidine-4-ylthiol RU2117659C1 (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
GB9202298.7 1992-02-04
GB929202298A GB9202298D0 (en) 1992-02-04 1992-02-04 Antibiotic compounds

Publications (2)

Publication Number Publication Date
RU93058253A true RU93058253A (en) 1996-12-27
RU2117659C1 RU2117659C1 (en) 1998-08-20

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RU93058253/04A RU2117659C1 (en) 1992-02-04 1993-02-02 Carbopenem derivatives, their pharmaceutically acceptable salts and hydrolyzed in vivo esters (variants), method of synthesis (variants), pharmaceutical composition showing antibacterial activity, derivatives of pyrrolidine-4-ylthiol and protected derivatives of pyrrolidine-4-ylthiol

Country Status (35)

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US (7) US5478820A (en)
EP (1) EP0579826B1 (en)
JP (1) JP2730600B2 (en)
KR (1) KR100200986B1 (en)
CN (1) CN1036006C (en)
AP (1) AP398A (en)
AT (1) ATE173262T1 (en)
AU (1) AU668133B2 (en)
CA (1) CA2106370C (en)
CZ (1) CZ286878B6 (en)
DE (2) DE69322007T2 (en)
DK (1) DK0579826T3 (en)
ES (1) ES2123654T3 (en)
FI (1) FI104074B1 (en)
GB (2) GB9202298D0 (en)
GE (1) GEP20022694B (en)
HK (1) HK1013998A1 (en)
HR (1) HRP930103B1 (en)
HU (3) HUT66514A (en)
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LU (1) LU90970I2 (en)
MY (1) MY111685A (en)
NL (1) NL300104I2 (en)
NO (2) NO304315B1 (en)
NZ (2) NZ272038A (en)
PL (3) PL174601B1 (en)
RU (1) RU2117659C1 (en)
SG (1) SG48817A1 (en)
SI (1) SI9300056B (en)
SK (1) SK280890B6 (en)
TW (1) TW408124B (en)
UA (1) UA44885C2 (en)
WO (1) WO1993015078A1 (en)
YU (1) YU48998B (en)
ZA (1) ZA93453B (en)

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