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1. 发明授权

US4331688A Therapeutic method for inhibiting gastric secretion by administration of 15-deoxy-16-hydroxy prostaglandins 失效
标题翻译：通过施用15-脱氧-16-羟基前列腺素来抑制胃分泌的治疗方法
公开(公告)号：US4331688A
公开(公告)日：1982-05-25
申请号：US215802
申请日：1980-12-12
申请人： Harold C. Kluender , Warren D. Woessner , William G. Biddlecom
发明人： Harold C. Kluender , Warren D. Woessner , William G. Biddlecom
IPC分类号： C07C29/09 , C07C29/147 , C07C29/36 , C07C29/42 , C07C29/62 , C07C45/45 , C07C45/62 , C07C47/293 , C07C47/30 , C07C49/293 , C07C49/433 , C07C49/443 , C07C51/09 , C07C51/353 , C07C51/38 , C07C61/04 , C07C61/08 , C07C405/00 , C07F1/08 , A61K31/12
CPC分类号： C07F1/08 , C07C29/095 , C07C29/147 , C07C29/36 , C07C29/42 , C07C29/62 , C07C405/0025 , C07C45/45 , C07C45/62 , C07C47/293 , C07C47/30 , C07C49/293 , C07C49/433 , C07C49/443 , C07C51/09 , C07C51/353 , C07C51/38 , C07C61/04 , C07C61/08 , C07B2200/07 , C07B2200/09 , C07C2101/04 , C07C2101/08 , C07C2101/14 , C07C2101/20 , C07C2102/20 , C07C2102/22
摘要： Analogues of PGE.sub.1 having the structural formula, ##STR1## in which J is R-hydroxymethylene or S-hydroxymethylene; R.sub.1 is hydrogen; R.sub.2 is hydrogen or together with R.sub.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.sub.3 is hydrogen or methyl, or together with R.sub.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.sub.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.sub.4 is hydrogen or methyl or together with R.sub.2 or R.sub.3 forms a cycloalkyl or bicycloalkyl or bicycloalkenyl as defined above, or together with R.sub.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.sub.5 is selected from the group consisting of hydrogen, straight-chain alkyl having from 1 to 3 carbon atoms or together with R.sub.4 forms a cycloalkyl as defined above; and R.sub.6 is hydrogen or straight-chain alkyl having from 1 to 3 carbon atoms are disclosed.PGE.sub.1 ester analogues of the above formula, limited to the structures wherein two of R.sub.2, R.sub.3 R.sub.4 and R.sub.5 form a cycloalkyl, lower alkylated cycloalkyl, bicycloalkyl or bicycloalkenyl are also disclosed.The prostaglandin analogues selectively produce bronchodilation and decrease gastric secretion in vivo.Methods of preparing the analogues and starting materials required in the synthesis of the analogues are also disclosed.
摘要翻译：具有结构式的PGE1的类似物，其中J是R-羟基亚甲基或S-羟基亚甲基; R1是氢; R2是氢或与R4一起是具有2至3个碳原子的亚甲基链，使得形成包含5至6个碳原子的环烷基; R 3为氢或甲基，或与R 4一起为亚甲基或2至5个碳原子的低级烷基化亚甲基链，使得形成包含4-7个碳原子的环烷基或低级烷基化环烷基，或与R4一起形成双环烷基或具有下式的双环烯基部分：，使得形成双环烷基或双环烯基化合物，其中m和n是0-3的整数，p是0-4的整数，q是整数具有1至4的值，并且其中双环烯基的双键位于m，n，p或q桥中; R4是氢或甲基，或与R2或R3一起形成如上定义的环烷基或双环烷基或双环烯基，或与R5一起形成3至5个碳原子的亚甲基链，使得形成包含4至6个碳原子的环烷基; R5选自氢，具有1至3个碳原子的直链烷基或与R 4一起形成如上定义的环烷基; 并且R6是氢或具有1至3个碳原子的直链烷基。还公开了上述式的PGE1酯类似物，其限于其中R2，R3R4和R5两个形成环烷基，低级烷基化环烷基，双环烷基或双环烯基的结构。前列腺素类似物选择性地产生支气管扩张并减少体内胃分泌。还公开了合成类似物所需的类似物和起始材料的方法。

2. 发明授权

US4275224A 15-Deoxy-16-hydroxy prostaglandins 失效
标题翻译： 15-脱氧-16-羟基前列腺素
公开(公告)号：US4275224A
公开(公告)日：1981-06-23
申请号：US973010
申请日：1978-12-26
申请人： Harold C. Kluender , Warren D. Woessner , William G. Biddlecom
发明人： Harold C. Kluender , Warren D. Woessner , William G. Biddlecom
IPC分类号： C07C29/09 , C07C29/147 , C07C29/36 , C07C29/42 , C07C29/62 , C07C45/45 , C07C45/62 , C07C47/293 , C07C47/30 , C07C49/293 , C07C49/433 , C07C49/443 , C07C51/09 , C07C51/353 , C07C51/38 , C07C61/04 , C07C61/08 , C07C405/00 , C07F1/08 , C07C177/00
CPC分类号： C07F1/08 , C07C29/095 , C07C29/147 , C07C29/36 , C07C29/42 , C07C29/62 , C07C405/00 , C07C405/0025 , C07C45/45 , C07C45/62 , C07C47/293 , C07C47/30 , C07C49/293 , C07C49/433 , C07C49/443 , C07C51/09 , C07C51/353 , C07C51/38 , C07C61/04 , C07C61/08 , C07B2200/07 , C07B2200/09 , C07C2101/04 , C07C2101/08 , C07C2101/14 , C07C2102/20 , C07C2102/22 , C07C2102/42
摘要： Analogues of PGE.sub.1 having the structural formula, ##STR1## in which J is R-hydroxymethylene or S-hydroxymethylene; R.sub.1 is hydrogen; R.sub.2 is hydrogen or together with R.sub.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.sub.3 is hydrogen or methyl, or together with R.sub.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.sub.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.sub.4 is hydrogen or methyl or together with R.sub.2 or R.sub.3 forms a cycloalkyl or bicycloalkyl or bicycloalkenyl as defined above, or together with R.sub.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.sub.5 is selected from the group consisting of hydrogen, straight-chain alkyl having from 1 to 3 carbon atoms or together with R.sub.4 forms a cycloalkyl as defined above; and R.sub.6 is hydrogen or straight-chain alkyl having from 1 to 3 carbon atoms are disclosed. PGE.sub.1 ester analogues of the above formula, limited to the structures wherein two of R.sub.2, R.sub.3, R.sub.4 and R.sub.5 form a cycloalkyl, lower alkylated cycloalkyl, bicycloalkyl or bicycloalkenyl are also disclosed.The prostaglandin analogues selectively produce bronchodilation and decrease gastric secretion in vivo.Methods of preparing the analogues and starting materials required in the synthesis of the analogues are also disclosed.
摘要翻译：具有结构式的PGE1的类似物，其中J是R-羟基亚甲基或S-羟基亚甲基; R1是氢; R2是氢或与R4一起是具有2至3个碳原子的亚甲基链，使得形成包含5至6个碳原子的环烷基; R 3为氢或甲基，或与R 4一起为亚甲基或2至5个碳原子的低级烷基化亚甲基链，使得形成包含4-7个碳原子的环烷基或低级烷基化环烷基，或与R4一起形成双环烷基或具有下式的双环烯基部分：，使得形成双环烷基或双环烯基化合物，其中m和n是0-3的整数，p是0-4的整数，q是整数具有1至4的值，并且其中双环烯基的双键位于m，n，p或q桥中; R4是氢或甲基，或与R2或R3一起形成如上定义的环烷基或双环烷基或双环烯基，或与R5一起形成3至5个碳原子的亚甲基链，使得形成包含4至6个碳原子的环烷基; R5选自氢，具有1至3个碳原子的直链烷基或与R 4一起形成如上定义的环烷基; 并且R6是氢或具有1至3个碳原子的直链烷基。还公开了上述式的PGE1酯类似物，限于其中R2，R3，R4和R5中两个形成环烷基，低级烷基化环烷基，双环烷基或双环烯基的结构。前列腺素类似物选择性地产生支气管扩张并减少体内胃分泌。还公开了合成类似物所需的类似物和起始材料的方法。

3. 发明授权

US4336404A 1-Acyloxy-15-deoxy-16-hydroxy-analogs of prostaglandin E.sub.1 失效
标题翻译：前列腺素E1的1-氧代-15-脱氧-16-羟基 - 类似物
公开(公告)号：US4336404A
公开(公告)日：1982-06-22
申请号：US154384
申请日：1980-05-29
申请人： William G. Biddlecom , Harold C. Kluender , Warren D. Woessner
发明人： William G. Biddlecom , Harold C. Kluender , Warren D. Woessner
IPC分类号： C07C405/00 , C07C69/18
CPC分类号： C07C405/0025
摘要： Disclosed are 1-acyloxy-15-deoxy-16-hydroxy prostaglandin E.sub.1 analogs characterized by the formula: ##STR1## Compounds corresponding to the foregoing formula in which R.sub.1 can be H or methyl and R.sub.2 can be C(CH.sub.3).sub.2 (CH.sub.2).sub.2 CH.sub.3 or (CH.sub.2).sub.3 CH.sub.3 are variously useful as inhibitors of gastric secretion and as bronchodilators.
摘要翻译：本发明公开了以下式表征的1-酰氧基-15-脱氧-16-羟基前列腺素E1类似物：其中R 1可以是H或甲基，R 2可以是C（CH 3）2（CH 2） 2CH3或（CH2）3CH3可用作胃分泌抑制剂和支气管扩张剂。

4. 发明授权

US4171331A 1 And 2-substituted analogues of certain prostaglandins 失效
标题翻译： 1和某些前列腺素的2-取代的类似物
公开(公告)号：US4171331A
公开(公告)日：1979-10-16
申请号：US912515
申请日：1978-06-05
申请人： William G. Biddlecom , Harold C. Kluender , Warren D. Woessner
发明人： William G. Biddlecom , Harold C. Kluender , Warren D. Woessner
IPC分类号： A01N57/18 , C07C45/56 , C07C45/59 , C07C45/63 , C07C45/67 , C07C49/707 , C07C405/00 , C07D295/116 , C07D295/24 , C07F9/40 , A01N9/36
CPC分类号： C07D295/24 , C07C309/00 , C07C405/00 , C07C405/0033 , C07C405/0041 , C07C45/56 , C07C45/59 , C07C45/63 , C07C45/673 , C07C49/707 , C07D295/116 , C07F9/4018
摘要： Disclosed are trans 1 & 2-di(loweralkyl)phosphono; 1 & 2-chloro, bromo and iodo; 1 & 2-thio and 1 & 2-amino analogues of E.sub.1, A.sub.1, F.sub.1.alpha., F.sub.1.beta., 11 deoxy E.sub.1, 11 deoxy F.sub.1.beta., and 11 deoxy F.sub.1.alpha. prostaglandins.The prostaglandins of this invention are variously useful as antithrombic agents, bronchodilators such as in the treatment of asthma, inhibitors of gastric secretion and as antihypertensive agents. Certain of the prostaglandins disclosed herein are useful as precursors for prostaglandins having one or more of the foregoing utilities.
摘要翻译：公开了反式1和2-二（低级烷基）膦酰基; 1＆2-氯，溴和碘; E1，A1，F1α，F1β，11脱氧E1，11脱氧F1β和11脱氧F1α前列腺素的1和2-硫代和1＆2-氨基类似物。

5. 发明授权

US4132738A Preparation of 15-deoxy-16-hydroxyprostaglandins 失效
标题翻译： 15-脱氧-16-羟基前列腺素的制备
公开(公告)号：US4132738A
公开(公告)日：1979-01-02
申请号：US880501
申请日：1978-02-23
申请人： Harold C. Kluender , Warren D. Woessner , William G. Biddlecom
发明人： Harold C. Kluender , Warren D. Woessner , William G. Biddlecom
IPC分类号： A61K31/557 , A61K31/20 , A61K31/5575 , A61P43/00 , B01J31/00 , C07C29/09 , C07C29/147 , C07C29/36 , C07C29/42 , C07C29/62 , C07C45/30 , C07C45/45 , C07C45/62 , C07C47/293 , C07C47/30 , C07C49/293 , C07C49/433 , C07C49/443 , C07C51/09 , C07C51/353 , C07C51/38 , C07C61/04 , C07C61/08 , C07C67/00 , C07C401/00 , C07C405/00 , C07F1/08 , C07C177/00
CPC分类号： C07F1/08 , C07C29/095 , C07C29/147 , C07C29/36 , C07C29/42 , C07C29/62 , C07C405/00 , C07C405/0025 , C07C45/305 , C07C45/45 , C07C45/62 , C07C47/293 , C07C47/30 , C07C49/293 , C07C49/433 , C07C49/443 , C07C51/09 , C07C51/353 , C07C51/38 , C07C61/04 , C07C61/08 , C07B2200/07 , C07B2200/09 , C07C2101/04 , C07C2101/08 , C07C2101/14 , C07C2102/20 , C07C2102/22 , C07C2102/42
摘要： Analogues of PGE.sub.1 having the structural formula, ##STR1## in which J is R-hydroxymethylene or S-hydroxymethylene; R.sub.1 is hydrogen; R.sub.2 is hydrogen or together with R.sub.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.sub.3 is hydrogen or methyl, or together with R.sub.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.sub.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.sub.4 is hydrogen or methyl or together with R.sub.2 or R.sub.3 forms a cycloalkyl or bicycloalkyl or bicycloalkenyl as defined above, or together with R.sub.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.sub.5 is selected from the group consisting of hydrogen, straight-chain alkyl having from 1 to 3 carbon atoms or together with R.sub.4 forms a cycloalkyl as defined above; and R.sub.6 is hydrogen or straight-chain alkyl having from 1 to 3 carbon atoms are disclosed.Pge.sub.1 ester analogues of the above formula, limited to the structures wherein two of R.sub.2, R.sub.3 R.sub.4 and R.sub.5 form a cycloalkyl, lower alkylated cycloalkyl, bicycloalkyl or bicycloalkenyl are also disclosed.The prostaglandin analogues selectively produce bronchodilation and decrease gastric secretion in vivo.Methods of preparing the analogues and starting materials required in the synthesis of the analogues are also disclosed.
摘要翻译：具有结构式的PGE1的类似物，其中J是R-羟基亚甲基或S-羟基亚甲基; R1是氢; R2是氢或与R4一起是具有2至3个碳原子的亚甲基链，使得形成包含5至6个碳原子的环烷基; R 3为氢或甲基，或与R 4一起为亚甲基或2至5个碳原子的低级烷基化亚甲基链，使得形成包含4-7个碳原子的环烷基或低级烷基化环烷基，或与R4一起形成双环烷基或具有下式的双环烯基部分：如图所示，形成双苄基或双环烷基化合物，其中M和N为具有0至3的值的整数，P为具有0至4的整数，Q为整数具有1至4的值，并且这些双子座的双键位于M，N，P或Q桥中; R4是氢或甲基，或与R2或R3一起形成如上定义的环烷基或双环烷基或双环烯基，或与R5一起形成3至5个碳原子的亚甲基链，使得形成包含4至6个碳原子的环烷基; R5选自氢，具有1至3个碳原子的直链烷基或与R 4一起形成如上定义的环烷基; 并且R6是氢或具有1至3个碳原子的直链烷基。

6. 发明授权

US4833157A Methods of inhibitng gastric secretion with prostaglandin derivatives 失效
标题翻译：用前列腺素衍生物抑制胃分泌的方法
公开(公告)号：US4833157A
公开(公告)日：1989-05-23
申请号：US140729
申请日：1988-01-04
申请人： Harold C. Kluender , Warren D. Woessner , William G. Biddlecom
发明人： Harold C. Kluender , Warren D. Woessner , William G. Biddlecom
IPC分类号： C07C29/09 , C07C29/147 , C07C29/36 , C07C29/42 , C07C29/62 , C07C45/30 , C07C45/45 , C07C45/62 , C07C47/293 , C07C47/30 , C07C49/293 , C07C49/433 , C07C49/443 , C07C51/09 , C07C51/353 , C07C51/38 , C07C61/04 , C07C61/08 , C07C405/00 , C07F1/08
CPC分类号： C07F1/08 , C07C29/095 , C07C29/147 , C07C29/36 , C07C29/42 , C07C29/62 , C07C405/00 , C07C405/0025 , C07C45/305 , C07C45/45 , C07C45/62 , C07C47/293 , C07C47/30 , C07C49/293 , C07C49/433 , C07C49/443 , C07C51/09 , C07C51/353 , C07C51/38 , C07C61/04 , C07C61/08 , C07B2200/07 , C07B2200/09 , C07C2101/04 , C07C2101/08 , C07C2101/14 , C07C2102/20 , C07C2102/22 , Y10S514/926 , Y10S514/927
摘要： A therapeutic method for inhibiting gastric secretion in an individual for whom such therapy is indicated is disclosed. The method comprises administering to such an individual an effective inhibitory amount of certain derivatives of 15-deoxy-16-hydroxy-prostaglandin E.sub.1 esters.
摘要翻译：公开了一种治疗方法，用于抑制表达这种治疗的个体中的胃分泌。该方法包括向这样的个体施用有效抑制量的15-脱氧-16-羟基 - 前列腺素E1酯的某些衍生物。

7. 发明授权

US4415592A 15-Deoxy-16-hydroxy prostaglandins for producing bronchodilation 失效
标题翻译：用于产生支气管扩张的15-脱氧-16-羟基前列腺素
公开(公告)号：US4415592A
公开(公告)日：1983-11-15
申请号：US357428
申请日：1982-03-12
申请人： Harold C. Kluender , Warren D. Woessner , William G. Biddlecom
发明人： Harold C. Kluender , Warren D. Woessner , William G. Biddlecom
IPC分类号： C07C29/09 , C07C29/147 , C07C29/36 , C07C29/42 , C07C29/62 , C07C45/45 , C07C45/62 , C07C47/293 , C07C47/30 , C07C49/293 , C07C49/433 , C07C49/443 , C07C51/09 , C07C51/353 , C07C51/38 , C07C61/04 , C07C61/08 , C07C405/00 , C07F1/08 , A61K31/12
CPC分类号： C07F1/08 , C07C29/095 , C07C29/147 , C07C29/36 , C07C29/42 , C07C29/62 , C07C405/0025 , C07C45/45 , C07C45/62 , C07C47/293 , C07C47/30 , C07C49/293 , C07C49/433 , C07C49/443 , C07C51/09 , C07C51/353 , C07C51/38 , C07C61/04 , C07C61/08 , C07B2200/07 , C07B2200/09 , C07C2101/04 , C07C2101/08 , C07C2101/14 , C07C2101/20 , C07C2102/20 , C07C2102/22
摘要： Analogues of PGE.sub.1 having the structural formula, ##STR1## in which J is R-hydroxymethylene or S-hydroxymethylene; R.sub.1 is hydrogen; R.sub.2 is hydrogen or together with R.sub.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.sub.3 is hydrogen or methyl, or together with R.sub.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.sub.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.sub.4 is hydrogen or methyl or together with R.sub.2 or R.sub.3 forms a cycloalkyl or bicycloalkyl or bicycloalkenyl as defined above, or together with R.sub.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.sub.5 is selected from the group consisting of hydrogen, straight-chain alkyl having from 1 to 3 carbon atoms or together with R.sub.4 forms a cycloalkyl as defined above; and R.sub.6 is hydrogen or straight-chain alkyl having from 1 to 3 carbon atoms are disclosed.PGE.sub.1 ester analogues of the above formula, limited to the structures wherein two of R.sub.2, R.sub.3, R.sub.4 and R.sub.5 form a cycloalkyl, lower alkylated cycloalkyl, bicycloalkyl or bicycloalkenyl are also disclosed.The prostaglandin analogues selectively produce bronchodilation and decrease gastric secretion in vivo.Methods of preparing the analogues and starting materials required in the synthesis of the analogues are also disclosed.
摘要翻译：具有结构式的PGE1的类似物，其中J是R-羟基亚甲基或S-羟基亚甲基; R1是氢; R2是氢或与R4一起是具有2至3个碳原子的亚甲基链，使得形成包含5至6个碳原子的环烷基; R 3为氢或甲基，或与R 4一起为亚甲基或2至5个碳原子的低级烷基化亚甲基链，使得形成包含4-7个碳原子的环烷基或低级烷基化环烷基，或与R4一起形成双环烷基或具有下式的双环烯基部分：，使得形成双环烷基或双环烯基化合物，其中m和n是0-3的整数，p是0-4的整数，q是整数具有1至4的值，并且其中双环烯基的双键位于m，n，p或q桥中; R4是氢或甲基，或与R2或R3一起形成如上定义的环烷基或双环烷基或双环烯基，或与R5一起形成3至5个碳原子的亚甲基链，使得形成包含4至6个碳原子的环烷基; R5选自氢，具有1至3个碳原子的直链烷基或与R 4一起形成如上定义的环烷基; 并且R6是氢或具有1至3个碳原子的直链烷基。还公开了上述式的PGE1酯类似物，限于其中R2，R3，R4和R5中两个形成环烷基，低级烷基化环烷基，双环烷基或双环烯基的结构。前列腺素类似物选择性地产生支气管扩张并减少体内胃分泌。还公开了合成类似物所需的类似物和起始材料的方法。

8. 发明授权

US4149017A Intermediates for the preparation of bicycloalkyl derivatives of prostaglandins 失效
标题翻译：用于制备前列腺素双环烷基衍生物的中间体
公开(公告)号：US4149017A
公开(公告)日：1979-04-10
申请号：US818995
申请日：1977-07-25
申请人： Warren D. Woessner , Charles J. Sih , Harold C. Kluender , Henry C. Arndt , William G. Biddlecom
发明人： Warren D. Woessner , Charles J. Sih , Harold C. Kluender , Henry C. Arndt , William G. Biddlecom
IPC分类号： A61K31/12 , A61K31/19 , A61K31/215 , A61K31/22 , A61K31/557 , A61P43/00 , C07C33/44 , C07C43/30 , C07C45/00 , C07C45/63 , C07C49/23 , C07C49/613 , C07C67/00 , C07C401/00 , C07C405/00 , C07D307/83
CPC分类号： C07D307/83 , C07C33/44 , C07C405/00 , Y02P20/55 , Y02P20/582
摘要： Useful intermediates in the preparation of bicycloalkyl analogues or derivatives of prostaglandins are represented by the formula ##STR1## wherein: X is an iodo or bromo radical;A is an acid-labile hydroxyl-protecting group;G is an integer having a value of from 0 to 10; andB is selected for the class of bicycloalkyl radicals of the formula: ##STR2## WHERE M AND P ARE INTEGERS HAVING A VALUE OF FROM 1 TO 4; N IS AN INTEGER HAVING A VALUE OF FROM 0 TO 4 SUCH THAT THE SUM OF M, N AND P IS GREATER THAN OR EQUAL TO 3 AND THE POINT OF ATTACHMENT OF THE ALKYL CHAIN (CH.sub.2).sub.g to the bicycloalkyl radical is in the (CH.sub.2).sub.m bridge or in the bridgehead position.
摘要翻译：制备双环烷基类似物或前列腺素衍生物的有用中间体由下式表示：其中：

9. 发明授权

US4127612A 19-Hydroxy PGE.sub.1 carbinol analogues 失效
标题翻译： 19-羟基PGE {HD 1 {B甲醇类似物
公开(公告)号：US4127612A
公开(公告)日：1978-11-28
申请号：US887666
申请日：1978-03-17
申请人： Harold C. Kluender , Warren D. Woessner
发明人： Harold C. Kluender , Warren D. Woessner
IPC分类号： C07C33/42 , C07C43/17 , C07C45/00 , C07C45/63 , C07C49/753 , C07C51/60 , C07C405/00 , C07F1/08 , C07C177/00
CPC分类号： C07F1/08 , C07C33/423 , C07C405/0025 , C07C43/17 , C07C45/00 , C07C45/63 , C07C49/753 , C07C51/60
摘要： 19-Hydroxy carbinol analogues of PGE.sub.1 having the structure ##STR1## are disclosed as bronchodilators. Methods of preparing the analogues are also disclosed.
摘要翻译：公开了具有结构的PGE1的19-羟基甲醇类似物作为支气管扩张剂。

10. 发明授权

US4138583A Cycloalkenyl analogues of prostaglandin F 失效
标题翻译：前列腺素F的环烯基类似物
公开(公告)号：US4138583A
公开(公告)日：1979-02-06
申请号：US803611
申请日：1977-06-06
申请人： Warren D. Woessner , William G. Biddlecom , Henry C. Arndt , George P. Peruzzotti , Charles J. Sih
发明人： Warren D. Woessner , William G. Biddlecom , Henry C. Arndt , George P. Peruzzotti , Charles J. Sih
IPC分类号： C07C405/00 , C07C177/00
CPC分类号： C07C405/00
摘要： Analogues of prostaglandins A, E, and F in which the C.sub.13 -C.sub.20 chain of the natural prostaglandins is replaced by a cycloalkenyl or a hydroxycycloalkenyl moiety such that vinylene radical and the hydroxyl group of the ring respectively retain their natural sequential positions at C.sub.13 -C.sub.14 and C.sub.15, inhibit aggregation of platelets in vitro and exhibit useful cardiovascular activity in vivo.
摘要翻译：前列腺素A，E和F的类似物，其中天然前列腺素的C13-C20链被环烯基或羟基环烯基部分代替，使得亚乙烯基和环的羟基分别在C13-C14保持其自然连续位置和C15，体外抑制血小板聚集，并在体内显示出有用的心血管活性。

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