Pliva, Farmaceutska, Kemijska, Prehrambena I Kozmeticka Industrija,

Pliva D.d.

Glaxosmithkline Istrazivacki Centar Zagreb D.o

Glaxosmithkline Istrazivacki Center Zagreb

Glaxosmithkline Istrazivacki Centar Zagreb D.o.o.

Nedjeljko Kujundzic

Gorjana Lazarevski

Gabrijela Kobrehel

Antun Hutinec

Sulejman Alihodzic

Karmen Brajsa

Miljenko Dumic

Andrea Fajdetic

Mirjana Bukvic Krajacic

Zeljko Kelneric

Zrinka Ivezic

Dina Pavlovic

Andrea Hasenohrl

The invention relates to substituted 9a-N-{N'-[4-(sulfonyl)phenyl]carbamoyl} derivatives of 9-deoxo-9-dihydro-9a-aza-9a-homoerithromycin A and 5-0-desosaminyl-9-deoxo-9-di-hydro-9a-aza-9a-homoerithronolide A, novel semisynthetic macrolide antibiotics of the azalide series general formula (1), wherein R represents H or cladinosyl moiety and R1 represents chloro, amino, phenylamino, 2-pyridylamino, 3,4-dimethyl-4-isoxalylamino and 5-methyl-3-isoxazolylamino group, and pharmaceutically acceptable addition salts thereof with inorganic or organic acids. to the process for their preparation of pharmaceutical composition as well as the use their compositions for sterilization rooms and medical instruments as well as for protection of wall and wooden coatings 

Substituted 9a-N-(N'-(sulfonyl)phenylcarbamoyl)derivatives of 9-deoxo-9-dihydro-9a-aza-9a-homoerithomycin A and 5-0-desosaminyl-9-deoxo-9-dihydro-9-a-aza-9a-homoerithronolide A

The invention relates to N&#x2033;-substituted 9a-N-(N'-carbamoyl-&#x3b3;-aminopropyl), 9a-N-(N&#x2032;-thiocarbamoyl-&#x3b3;-aminopropyl), 9a-N-[N&#x2032;-&#x3b2;-cyanoethyl)-N&#x2032;-carbamoyl-&#x3b3;-aminopropyl] and 9a-N-[N&#x2032;-&#x3b2;-cyanoethyl)-N&#x2032;-thiocarbamoyl-&#x3b3;-am inopropyl] derivatives of 9-deoxo-9-dihydro-9a-aza-9a-homoerithromycin A and 5-O-desosaminyl-9-deoxo-9-dihydro-9a-aza-9a-homoerithronolide A, novel semi-synthetic macrolide antibiotics of the azalide series, of the general formula 1, wherein R represents H or cladinosyl moiety, Rrepresents H or &#x3b2;-cyanoethyl moiety, Rrepresents isopropyl, 1-naphtyl, 2-naphtyl, benzyl, 2-(trifluoromethyl)phenyl, 3-phenylpropyl, &#x3b2;-phenylethyl, ethoxycarbonyl-methyl, 1-(1-naphtyl)ethyl, 3,4,5-trimethoxyphenyl and 2,4-dichlorophenyl group, and X represents O and S, and their acceptable addition salts thereof with inorganic or organic acids, to the process for preparation of their pharmaceutical compositions as well as the use their compositions in the treatment of bacterial infections.

Semisynthetic macrolide antibiotics of the azalide series

9a-N-[N'-(phenylsulfonyl)carbamoyl] derivatives of 9-deoxo-9-dihydro-9a-aza-9a-homoerythromycin A and of 5-O-desosaminyl-9-deoxo-9-dihydro-9a-aza-9a-homoerythronolide A and their pharmaceutically acceptable addition salts with inorganic or organic acids are provided, along with a process for their preparation, pharmaceutical compositons, and use in treating bacterial infections.

9a-N-[N'-(phenylsulfonyl)carbamoyl] derivatives of 9-deoxo-9-dihydro-9a-aza-9a-homoerythromycin A and of 5-O-desosaminyl-9-deoxo-9-dihydro-9a-aza-9a-homoerythronolide A

The present invention relates to .beta.,.beta.-disubstituted derivatives of 9-deoxo-9a-N-ethenyl-9a-aza-9a-homoerythromycin A, new semisynthetic antibiotics of macrolide class of the general formula (I) ##STR1## wherein R.sup.1 and R.sup.2 are mutually the same or different and represent nitrile, carboxy group of the formula COOR.sup.3, wherein R.sup.3 represents C.sub.1 -C.sub.4 alkyl group, or keto group of the formula COR.sup.4, wherein R.sup.4 represents C.sub.1 -C.sub.4 alkyl group, to their pharmaceutically acceptable addition salts with inorganic or organic acids, to a process for the preparation thereof, to a process for the preparation of pharmaceutical compositions, as well as to the use of the obtained pharmaceutical compositions in the treatment of bacterial infections.

.beta.,.beta.-distributed derivatives of

The invention relates to 9-N-ethenyl derivatives of 9 (S)-erythromycylamine, new semisynthetic antibiotics of the macrolide class of the general formula (I) ##STR1## wherein R.sup.1 and R.sup.2 are the same or different and represent nitryl, a carboxyl group of the formula COOR.sup.3, wherein R.sup.3 represents a C.sub.1 -C.sub.4 alkyl group, or a keto group of the formula COR.sup.4, wherein R.sup.4 represents a C.sub.1 -C.sub.4 alkyl group, to their pharmaceutically acceptable addition salts with inorganic or organic acids, to a process for their preparation, to a process for the preparation of the pharmaceutical compositions as well as to the use of the obtained pharmaceutical compositions in the treatment of bacterial infections.

9-N-ethenyl derivatives of 9(S)-erythromycylamine

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Zagreb, Croatia

Nedjeljko Kujundzic