公开(公告)号：EP0484030A2

公开(公告)日：1992-05-06

申请号：EP91309725.9

申请日：1991-10-21

申请人： Bristol-Myers Squibb Company

发明人： Hudyma, Thomas W. ,  Partyka, Richard A.

IPC分类号： C07D501/20 ,  C07D501/18 ,  C07D463/00 ,  A61K31/545 ,  A61K31/435

CPC分类号： C07D501/00 ,  Y02P20/55

摘要： A compound of formula I

wherein

X is sulfur or CH2;
R 1 is hydrogen, hydroxy, amino, C 1-6 alkyl, C 2-6 alkenyl, C 2-6 alkynyl, phenyl optionally substituted with one to three C 1-6 alkyl, C 1-6 alkyloxy or hydroxy, C 1-6 alkylthio, phenylthio optionally substituted with one to three C 1-6 alkyl or C 1-6 alkyloxy on the phenyl ring, phenylmethyloxy optionally substituted with one to three C 1-6 alkyl or C 1-6 alkyloxy on the phenyl ring, 1-morpholino, C 1-6 alkyloxy, C 2-6 alkenylmethyloxy, C 3-6 alkynylmethyloxy, C 1-6 alkylamino, C 1-6 dialkylamino or a radical selected from the group consisting of
and

in which n is 0 to 3, R 5 is C 1-6 alkyl or hydrogen, and R 3 and R 4 are independently C 1-6 alkyl ;
R 2 is hydrogen, a conventional amino protecting group or an acyl group ;
R° is hydrogen or a conventional carboxy protecting group, or -CO Z R° taken together forms a physiologically hydrolyzable ester; or
pharmaceutically acceptable salts or solvates thereof.

摘要翻译： 式I化合物其中X是硫或CH2; R 1是氢，羟基，氨基，C 1-6烷基，C 2-6烯基，C 2-6炔基，任选地被一至三个C 1-6烷基，C 1-6烷氧基或羟基，C 1-6烷硫基， 任选被苯基环上一至三个C 1-6烷基或C 1-6烷氧基取代的苯硫基，苯基环上任选被一至三个C 1-6烷基或C 1-6烷氧基取代的苯基甲氧基，1-吗啉代，C 1-6烷氧基 ，C 2-6烯基甲氧基，C 3-6炔基甲氧基，C 1-6烷基氨基，C 1-6二烷基氨基或选自下组的基团，其中n为0至3，R 5为C 1-6烷基或 氢，R 3和R 4独立地是C 1-6烷基; R 2是氢，常规的氨基保护基或酰基; R DEG是氢或常规的羧基保护基，或-CO 2 R 2一起形成生理上可水解的酯; 或其药学上可接受的盐或溶剂化物。 婷

公开(公告)号：EP0484030A3

公开(公告)日：1992-08-12

申请号：EP91309725.9

申请日：1991-10-21

申请人： Bristol-Myers Squibb Company

发明人： Hudyma, Thomas W. ,  Partyka, Richard A.

IPC分类号： C07D501/20 ,  C07D501/18 ,  C07D463/00 ,  A61K31/545 ,  A61K31/435

CPC分类号： C07D501/00 ,  Y02P20/55

摘要： A compound of formula I

wherein
X is sulfur or CH2; R 1 is hydrogen, hydroxy, amino, C 1-6 alkyl, C 2-6 alkenyl, C 2-6 alkynyl, phenyl optionally substituted with one to three C 1-6 alkyl, C 1-6 alkyloxy or hydroxy, C 1-6 alkylthio, phenylthio optionally substituted with one to three C 1-6 alkyl or C 1-6 alkyloxy on the phenyl ring, phenylmethyloxy optionally substituted with one to three C 1-6 alkyl or C 1-6 alkyloxy on the phenyl ring, 1-morpholino, C 1-6 alkyloxy, C 2-6 alkenylmethyloxy, C 3-6 alkynylmethyloxy, C 1-6 alkylamino, C 1-6 dialkylamino or a radical selected from the group consisting of
and

in which n is 0 to 3, R 5 is C 1-6 alkyl or hydrogen, and R 3 and R 4 are independently C 1-6 alkyl ; R 2 is hydrogen, a conventional amino protecting group or an acyl group ; R° is hydrogen or a conventional carboxy protecting group, or -CO Z R° taken together forms a physiologically hydrolyzable ester; or pharmaceutically acceptable salts or solvates thereof.

公开(公告)号：EP0727426A2

公开(公告)日：1996-08-21

申请号：EP96400295.0

申请日：1996-02-13

申请人： BRISTOL-MYERS SQUIBB COMPANY

发明人： Kim, Choung U. ,  Misco, Peter F. ,  Wichtowski, John A. ,  Ueda, Yasutsugu ,  Hudyma, Thomas W. ,  Matiskella, John D. ,  D'Andrea, Stanley W. ,  Hoeft, Shelley E. ,  Miller, Raymond F. ,  Mansuri, Muzammil M. ,  Bronson, Joanne J.

IPC分类号： C07D501/36 ,  A61K31/545

CPC分类号： C07D501/00

摘要： Novel cephem derivatives represented by the general formula

in which the Acyl substituent is a group of the formula

wherein Ar is a lipophilic optionally substituted phenyl, naphthyl, pyridyl or benzthiazolyl group; R 1 is selected from certain optionally substituted aliphatic, aromatic, arylaliphatic or sugar moieties and R 2 and R 3 are each independently hydrogen, alkyl or aminoalkylcarbonylamino are gram-positive antibacterial agents, especially useful in the treatment of infectious diseases caused by methicillin-resistant Staphylococcus aureus (MRSA).

摘要翻译： 由通式表示的新型头孢烯衍生物，其中酰基取代基是下式的基团其中Ar是亲脂性的任选取代的苯基，萘基，吡啶基或苯并噻唑基; R1选自某些任选取代的脂族，芳族，芳基脂族或糖部分，R2和R3各自独立地为氢，烷基或氨基烷基羰基氨基为革兰氏阳性抗菌剂，特别用于治疗由耐甲氧西林金黄色葡萄球菌引起的感染性疾病 MRSA）。

公开(公告)号：EP0727426A3

公开(公告)日：1996-10-23

申请号：EP96400295.0

申请日：1996-02-13

申请人： BRISTOL-MYERS SQUIBB COMPANY

发明人： Kim, Choung U. ,  Misco, Peter F. ,  Wichtowski, John A. ,  Ueda, Yasutsugu ,  Hudyma, Thomas W. ,  Matiskella, John D. ,  D'Andrea, Stanley W. ,  Hoeft, Shelley E. ,  Miller, Raymond F. ,  Mansuri, Muzammil M. ,  Bronson, Joanne J.

IPC分类号： C07D501/36 ,  A61K31/545

CPC分类号： C07D501/00

摘要： Novel cephem derivatives represented by the general formula

in which the Acyl substituent is a group of the formula

wherein Ar is a lipophilic optionally substituted phenyl, naphthyl, pyridyl or benzthiazolyl group; R 1 is selected from certain optionally substituted aliphatic, aromatic, arylaliphatic or sugar moieties and R 2 and R 3 are each independently hydrogen, alkyl or aminoalkylcarbonylamino are gram-positive antibacterial agents, especially useful in the treatment of infectious diseases caused by methicillin-resistant Staphylococcus aureus (MRSA).