专利号:US-4331688-A 优先权日:1978-02-23 标题 :Therapeutic method for inhibiting gastric secretion by administration of 15-deoxy-16-hydroxy prostaglandins 发明人:KLUENDER HAROLD C; WOESSNER WARREN D; BIDDLECOM WILLIAM G 权利人:MILES LAB 摘要:Analogues of PGE 1 having the structural formula, ##STR1## in which J is R-hydroxymethylene or S-hydroxymethylene; R 1 is hydrogen; R 2 is hydrogen or together with R 4 is a methylene chain of 2 to 3 carbon atoms such that a cycloalkyl of 5 to 6 carbon atoms inclusive is formed; R 3 is hydrogen or methyl, or together with R 4 is a methylene or a lower alkylated methylene chain of 2 to 5 carbon atoms such that a cycloalkyl or a lower alkylated cycloalkyl of 4 to 7 carbon atoms inclusive is formed, or together with R 4 is bicycloalkyl or bicycloalkenyl moiety having the formula: ##STR2## such that a bicycloalkyl or bicycloalkenyl compound is formed, wherein m and n are integers having a value from 0 to 3, p is an integer having a value from 0 to 4 and q is an integer having a value of from 1 to 4 and wherein the double bond of such bicycloalkenyl is in the m, n, p, or q bridge; R 4 is hydrogen or methyl or together with R 2 or R 3 forms a cycloalkyl or bicycloalkyl or bicycloalkenyl as defined above, or together with R 5 is a methylene chain of 3 to 5 carbon atoms such that a cycloalkyl of 4 to 6 carbon atoms inclusive is formed; R 5 is selected from the group consisting of hydrogen, straight-chain alkyl having from 1 to 3 carbon atoms or together with R 4 forms a cycloalkyl as defined above; and R 6 is hydrogen or straight-chain alkyl having from 1 to 3 carbon atoms are disclosed. n PGE 1 ester analogues of the above formula, limited to the structures wherein two of R 2 , R 3 R 4 and R 5 form a cycloalkyl, lower alkylated cycloalkyl, bicycloalkyl or bicycloalkenyl are also disclosed. n The prostaglandin analogues selectively produce bronchodilation and decrease gastric secretion in vivo. n Methods of preparing the analogues and starting materials required in the synthesis of the analogues are also disclosed.
专利号:US-4132738-A 优先权日:1978-02-23 标 题:Preparation of 15-deoxy-16-hydroxyprostaglandins 发明人:KLUENDER HAROLD C; WOESSNER WARREN D; BIDDLECOM WILLIAM G 权利人:MILES LAB 摘要:Analogues of PGE 1 having the structural formula, ##STR1## in which J is R-hydroxymethylene or S-hydroxymethylene; R 1 is hydrogen; R 2 is hydrogen or together with R 4 is a methylene chain of 2 to 3 carbon atoms such that a cycloalkyl of 5 to 6 carbon atoms inclusive is formed; R 3 is hydrogen or methyl, or together with R 4 is a methylene or a lower alkylated methylene chain of 2 to 5 carbon atoms such that a cycloalkyl or a lower alkylated cycloalkyl of 4 to 7 carbon atoms inclusive is formed, or together with R 4 is bicycloalkyl or bicycloalkenyl moiety having the formula: ##STR2## SUCH THAT A BICYCLOALKYL OR BICYCLOALKENYL COMPOUND IS FORMED, WHEREIN M AND N ARE INTEGERS HAVING A VALUE FROM 0 TO 3, P IS AN INTEGER HAVING A VALUE FROM 0 TO 4 AND Q IS AN INTEGER HAVING A VALUE OF FROM 1 TO 4 AND WHEREIN THE DOUBLE BOND OF SUCH BICYCLOALKENYL IS IN THE M, N, P, OR Q BRIDGE; R 4 is hydrogen or methyl or together with R 2 or R 3 forms a cycloalkyl or bicycloalkyl or bicycloalkenyl as defined above, or together with R 5 is a methylene chain of 3 to 5 carbon atoms such that a cycloalkyl of 4 to 6 carbon atoms inclusive is formed; R 5 is selected from the group consisting of hydrogen, straight-chain alkyl having from 1 to 3 carbon atoms or together with R 4 forms a cycloalkyl as defined above; and R 6 is hydrogen or straight-chain alkyl having from 1 to 3 carbon atoms are disclosed. n Pge 1 ester analogues of the above formula, limited to the structures wherein two of R 2 , R 3 R 4 and R 5 form a cycloalkyl, lower alkylated cycloalkyl, bicycloalkyl or bicycloalkenyl are also disclosed. n The prostaglandin analogues selectively produce bronchodilation and decrease gastric secretion in vivo. n Methods of preparing the analogues and starting materials required in the synthesis of the analogues are also disclosed.
专利号:US-4415592-A 优先权日:1978-02-23 标 题 :15-Deoxy-16-hydroxy prostaglandins for producing bronchodilation 发明人:KLUENDER HAROLD C; WOESSNER WARREN D; BIDDLECOM WILLIAM G 权利人:MILES LAB 摘要:Analogues of PGE 1 having the structural formula, ##STR1## in which J is R-hydroxymethylene or S-hydroxymethylene; R 1 is hydrogen; R 2 is hydrogen or together with R 4 is a methylene chain of 2 to 3 carbon atoms such that a cycloalkyl of 5 to 6 carbon atoms inclusive is formed; R 3 is hydrogen or methyl, or together with R 4 is a methylene or a lower alkylated methylene chain of 2 to 5 carbon atoms such that a cycloalkyl or a lower alkylated cycloalkyl of 4 to 7 carbon atoms inclusive is formed, or together with R 4 is bicycloalkyl or bicycloalkenyl moiety having the formula: ##STR2## such that a bicycloalkyl or bicycloalkenyl compound is formed, wherein m and n are integers having a value from 0 to 3, p is an integer having a value from 0 to 4 and q is an integer having a value of from 1 to 4 and wherein the double bond of such bicycloalkenyl is in the m, n, p, or q bridge; R 4 is hydrogen or methyl or together with R 2 or R 3 forms a cycloalkyl or bicycloalkyl or bicycloalkenyl as defined above, or together with R 5 is a methylene chain of 3 to 5 carbon atoms such that a cycloalkyl of 4 to 6 carbon atoms inclusive is formed; R 5 is selected from the group consisting of hydrogen, straight-chain alkyl having from 1 to 3 carbon atoms or together with R 4 forms a cycloalkyl as defined above; and R 6 is hydrogen or straight-chain alkyl having from 1 to 3 carbon atoms are disclosed. n PGE 1 ester analogues of the above formula, limited to the structures wherein two of R 2 , R 3 , R 4 and R 5 form a cycloalkyl, lower alkylated cycloalkyl, bicycloalkyl or bicycloalkenyl are also disclosed. n The prostaglandin analogues selectively produce bronchodilation and decrease gastric secretion in vivo. n Methods of preparing the analogues and starting materials required in the synthesis of the analogues are also disclosed.
专利号:US-4275224-A 优先权日:1978-02-23 标题:15-Deoxy-16-hydroxy prostaglandins 发明人:KLUENDER HAROLD C; WOESSNER WARREN D; BIDDLECOM WILLIAM G 权利人:MILES LAB 摘要:Analogues of PGE 1 having the structural formula, ##STR1## in which J is R-hydroxymethylene or S-hydroxymethylene; R 1 is hydrogen; R 2 is hydrogen or together with R 4 is a methylene chain of 2 to 3 carbon atoms such that a cycloalkyl of 5 to 6 carbon atoms inclusive is formed; R 3 is hydrogen or methyl, or together with R 4 is a methylene or a lower alkylated methylene chain of 2 to 5 carbon atoms such that a cycloalkyl or a lower alkylated cycloalkyl of 4 to 7 carbon atoms inclusive is formed, or together with R 4 is bicycloalkyl or bicycloalkenyl moiety having the formula: ##STR2## such that a bicycloalkyl or bicycloalkenyl compound is formed, wherein m and n are integers having a value from 0 to 3, p is an integer having a value from 0 to 4 and q is an integer having a value of from 1 to 4 and wherein the double bond of such bicycloalkenyl is in the m, n, p, or q bridge; R 4 is hydrogen or methyl or together with R 2 or R 3 forms a cycloalkyl or bicycloalkyl or bicycloalkenyl as defined above, or together with R 5 is a methylene chain of 3 to 5 carbon atoms such that a cycloalkyl of 4 to 6 carbon atoms inclusive is formed; R 5 is selected from the group consisting of hydrogen, straight-chain alkyl having from 1 to 3 carbon atoms or together with R 4 forms a cycloalkyl as defined above; and R 6 is hydrogen or straight-chain alkyl having from 1 to 3 carbon atoms are disclosed. PGE 1 ester analogues of the above formula, limited to the structures wherein two of R 2 , R 3 , R 4 and R 5 form a cycloalkyl, lower alkylated cycloalkyl, bicycloalkyl or bicycloalkenyl are also disclosed. n The prostaglandin analogues selectively produce bronchodilation and decrease gastric secretion in vivo. n Methods of preparing the analogues and starting materials required in the synthesis of the analogues are also disclosed.
专利号:US-2014315720-A1 优先权日:2012-10-24 标 题 :Polysaccharide ester microspheres and methods and articles relating thereto 发明人:FALLON DENIS G; GARRETT THOMAS S; KIZER LAWTON E; ZAZZARA KAREN L; COMBS MICHAEL T; JOHNSON RICHARD K; DEHART GARY 权利人:CELANESE ACETATE LLC 摘要:A method for producing a polysaccharide ester microsphere may include forming a polysaccharide ester product from a polysaccharide synthesis, wherein the polysaccharide ester product comprises a polysaccharide ester and a solvent; diluting the polysaccharide ester product, thereby yielding a polysaccharide ester dope; and forming a plurality of polysaccharide ester microspheres from the polysaccharide ester dope. Suitable polysaccharides may include, but are not limited to, starch, cellulose, hemicellulose, algenates, chitosan, and any combination thereof. Esters thereof may be organic esters (e.g., acetate and the like), inorganic esters (e.g., sulfonates and the like), or combinations thereof. Further, the solids conent of the polysaccharide ester dope, in some instances, may be greater than about 16 wt %.
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合成参考文献
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