专利号:US-4171439-A 优先权日:1975-04-11 标 题 :Antibacterial analogs of isocephalosporins 发明人:CONWAY TERRY T; LIM GARY M F; MENARD MARCEL 权利人:BRISTOL MYERS CO 摘要:There is described the stereoselective total synthesis of novel DELTA 2,3-1,4-morpholine-2-carboxylic acids possessing a fused beta -lactam ring in the 1,6-position and carrying a substituent cis to carbon 5 in the 7-position of the fused ring system represented by the general formula I wherein Z is halo or hydroxyl and X is acylamino. Also included in the invention are compounds of the above formula in which the carboxyl group at the 2-position is protected as by an easily cleavable ester group and salts of both the free acids and carboxyl-protected compounds. The compounds are potent antibacterial agents.
专利号:US-3822289-A 优先权日:1972-04-17 标题:Synthesis of thiophens 发明人:CLARK N; WEBSTER W 权利人:SYNTHETIC CHEMICALS LTD 摘要:THIOPENS ARE MADE BY REACTING ORGANIC COMPOUNDS HAVING A CONSECUTIVE CHAIN OF AT LEAST FOUR CARBON ATOMS WITH CARBON DISULPHIDE OR CARBONYL SULPHIDE IN A VAPOR PHASE REACTION IN THE PRESENCE OF A CATALYST.
专利号:US-7320993-B1 优先权日:1997-12-17 标题 :Aryl-substituted pyridylalkane, alkene, and alkine carboxamides useful as cytostatic useful as cytostatic and immuosuppressive agents 发明人:BIEDERMANN ELFI; HASMANN MAX; LOESER ROLAND; RATTEL BENNO; REITER FRIEDEMANN; SCHEIN BARBARA; SEIBEL KLAUS; VOGT KLAUS; WOSIKOWSKI KATJA; SCHEMAINDA ISABEL 权利人:ASTELLAS DEUTSCHLAND GMBH 摘要:The invention relates to new pyridylalkane, alkene, and alkine acid amides substituted with an aryl and/or heteroaryl residue according to the general formula (I), with a saturated or one or several-fold unsaturated hydrocarbon residue in the carboxylic acid group, methods for the synthesis of these compounds, medicaments containing these and their production as well as their therapeutic use, especially as cytostatic agents and immunosuppressive agents, for example in the treatment or prevention of various types of tumors and control of immune reactions such as autoimmune diseases.
专利号:US-4112230-A 优先权日:1975-04-11 标题 :Δ2,3 -1,4 Morpholine-2-carboxylic acid derivatives as antibacterial agents 发明人:MENARD MARCEL; LIM GARY M F; CONWAY TERRY T 权利人:BRISTOL MYERS CO 摘要:There is described the stereoselective total synthesis of novel DELTA 2,3-1,4-morpholine-2-carboxylic acids possessing a fused beta -lactam ring in the 1,6-position and carrying a substituent cis to carbon 5 in the 7-position of the fused ring system represented by the general formula I wherein Z is halo, hydroxyl, etherified hydroxyl or hydroxyl esterified with a carboxylic acid residue or a sulfonic acid residue and X is amino, azido or acylamino. Also included in the invention are compounds of formula I in which the carboxyl group at the 2-position is protected as by an easily cleavable ester group and salts of both the free acids and carboxyl-protected compounds of formula I. The compounds of formula I are potent antibacterial agents or are of use as intermediates in the preparation of such antibacterial agents.
专利号:US-4118566-A 优先权日:1975-07-23 标 题:Δ2,3 -1,4-Morpholine-2-carboxylic acid derivatives as antibacterial agents 发明人:HORNING DONALD E; MORRIS LEESON R; DOUGLAS JAMES L 权利人:BRISTOL MYERS CO 摘要:There is described the stereoselective total synthesis of novel DELTA 2,3-1,4-morpholine-2-carboxylic acids possessing a fused beta -lactam ring in the 1,6-position and carrying a substituent cis to carbon 5 in the 7-position of the fused ring system represented by the general formula I wherein X is amino, azido or acylamido and Z represents optionally substituted C1-C6 alkyl, aryl, aralkyl or heterocyclic. Also included in the invention are compounds of formula I in which the carboxyl group at the 2-position is protected as by an easily cleavable ester group and salts of both the free acids and carboxyl-protected compounds of formula I. The compounds of formula I are potent antibacterial agents or are of use as intermediates in the preparation of such antibacterial agents.
专利号:US-4166906-A 优先权日:1975-04-11 标题:0-2-Isocephem-4-carboxylic acid derivatives as antibacterial agents 发明人:CONWAY TERRY T; LIM GARY M F; MENARD MARCEL 权利人:BRISTOL MYERS CO 摘要:There is described the stereoselective total synthesis of novel DELTA 2,3-1,4-morpholine-2-carboxylic acids possessing a fused beta -lactam ring in the 1,6-position and carrying a substituent cis to carbon 5 in the 7-position of the fused ring system represented by the general formula I wherein Z is hydroxyl esterified with a sulfonic acid residue and X is acylamino. Also included in the invention are compounds of the above formula in which the carboxyl group of the 2-position is protected as by an easily cleavable ester group and salts of both the free acids and carboxyl-protected compounds. The compounds are potent antibacterial agents.