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3. 发明授权

US4430345A Prostaglandins 失效
标题翻译：前列腺素
公开(公告)号：US4430345A
公开(公告)日：1984-02-07
申请号：US431554
申请日：1982-09-30
申请人： Robert L. Jones , Norman H. Wilson
发明人： Robert L. Jones , Norman H. Wilson
IPC分类号： B29C47/04 , A61K31/19 , A61K31/557 , A61P7/02 , A61P11/00 , B65D33/25 , C07C41/48 , C07C43/315 , C07C45/44 , C07C59/11 , C07C59/13 , C07C59/147 , C07C59/205 , C07C59/31 , C07C59/325 , C07C59/46 , C07C59/54 , C07C59/62 , C07C59/74 , C07C59/80 , C07C59/86 , C07C67/00 , C07C69/608 , C07C69/675 , C07C69/716 , C07C69/732 , C07C69/738 , C07C231/00 , C07C233/08 , C07C235/30 , C07C235/78 , C07C251/42 , C07C251/50 , C07C251/52 , C07C251/54 , C07C253/00 , C07C255/31 , C07C301/00 , C07C311/51 , C07C323/12 , C07C405/00 , C07D213/63 , C07D307/60 , C07D307/93 , C07C131/02 , C07C131/08
CPC分类号： C07C255/00 , C07C405/0091 , C07C41/48 , C07C43/315 , C07C45/44 , C07C59/13 , C07C59/147 , C07C59/31 , C07C59/325 , C07C59/46 , C07C59/54 , C07C59/62 , C07C59/74 , C07C59/80 , C07C59/86 , C07D307/60 , C07D307/93 , C07B2200/07 , C07C2102/42 , Y10S514/826
摘要： Novel bicyclo [2,2,1] heptanes and hept-2Z-enes are substituted at the 5-position by a 6-carboxyhex-2-enyl group or a modification thereof, and at the 6-position by an aldoxime or ketoxime group which is O-substituted by an aliphatic hydrocarbon residue, an aromatic residue, or an aliphatic hydrocarbon residue substituted directly or through an oxygen or sulphur atom by an aromatic residue. Such compounds may be prepared by the action of an oximating agent on an intermediate which is substituted at the 6-position by an aldehydic or ketonic carbonyl group. The compounds are of value for use in pharmaceutical compositions particularly in the context of the inhibition of thromboxane activity.

5. 发明授权

US4837234A Prostaglandins 失效
标题翻译：前列腺素
公开(公告)号：US4837234A
公开(公告)日：1989-06-06
申请号：US869735
申请日：1986-07-22
申请人： Robert L. Jones , Norman H. Wilson
发明人： Robert L. Jones , Norman H. Wilson
IPC分类号： C07C43/315 , C07C45/44 , C07C59/62 , C07C405/00 , C07D493/08
CPC分类号： C07D493/08 , C07C255/00 , C07C405/0041 , C07C405/0091 , C07C43/315 , C07C45/44 , C07C59/62
摘要： Novel compounds have a formula (I) ##STR1## wherein ##STR2## represents a bicyclo [2,2,1] hept-2Z-ene, bicyclo [2,2,1] heptane, 7-oxa-bicyclo [2,2,1] hept-2Z-ene, 7-oxa-bicyclo [2,2,1] heptane, bicyclo [2,2,2] oct-2Z-ene or bicyclo [2,2,2] octane substituted at the 5-position by the group R.sup.1 and at the 6-position by the group ANR.sup.2 R, a 6,6-dimethyl-bicyclo [3,1,1] heptane substituted at the 2-position by the group R.sup.1 and at the 3-position by the group ANR.sup.2 R or at the 2-position by the group ANR.sup.2 R and at the 3-position by the group R.sup.1, a cyclohex-1-ene or cyclohexane substituted at the 4-position by the group R.sup.1 and at the 5-position by the group ANR.sup.2 R or a 1-hydroxycyclopentane substituted at the 2-position by the group R.sup.1 and at the 2-position by the group ANR.sup.2 R, R.sup.1 is a 6-carboxyhex-2-enyl group or a modification thereof as defined herein; A is an unbranched or branched aliphatic hydrocarbon group with a chain length between the points of attachment to the divalent cyclic group and to the group NR.sup.2 R of 1 to 5 carbon atoms or such a group substituted by an aromatic group; R.sup.2 is hydrogen, an aliphatic hydrocarbon group, an aromatic group or an aliphatic hydrocarbon group substituted by an aromatic group or groups; and R is a group --CO.NR.sup.3 R.sup.4, --CS.NR.sup.3 R.sup.4, --CNH.NR.sup.3 R.sup.4, --CO.R.sup.4 or --CS.R.sup.4 in which R.sup.3 is hydrogen, an aliphatic hydrocarbon group, an aromatic group or an aliphatic hydrocarbon group substituted by an aromatic group or groups, and R.sup.4 is an aliphatic hydrocarbon group, an aromatic group or an aliphatic hydrocarbon group substituted directly by an aromatic group or groups and/or through an oxygen or sulphur atom either by an aromatic group or by an aliphatic hydrocarbon group substituted directly by an aromatic group or groups. The compounds are of value for use in pharmaceutical compositions particularly in the context of the inhibition of thromboxane activity.
摘要翻译：新化合物具有式（I）其中表示双环[2,2,1]庚-2Z-烯，双环[2,2,1]庚烷，7-氧杂双环[ 2,2,1]庚-2Z-烯，7-氧杂双环[2,2,1]庚烷，双环[2,2,2]辛-2Z-烯或双环[2,2,2]辛烷取代在R5位置的5位和ANR2R基的6位，6位二甲基 - 双环[3,1,1]庚烷在2位被R1和3位取代 - 由ANR2R基团或在ANR2R基团的2位上，在3位被R1基团取代，在4-位上被R1基团取代的环己-1-烯或环己烷，位置由ANR2R基团或1-位羟基环戊烷在2-位被基团R1取代，2-位被ANR2R基团取代，R1是如本文所定义的6-羧基己-2-烯基或其修饰; A是与二价环状基团连接的点与1〜5个碳原子的基团NR2R之间的链长的非支链或支链脂族烃基，或者被芳基取代的基团; R2是氢，脂族烃基，芳香族基团或被芳族基团取代的脂族烃基; 并且R是基团-CO.NR 3 R 4，-CS.NR 3 R 4，-CNH.NR 3 R 4，-CO.R 4或-CS.R 4，其中R 3是氢，脂族烃基，芳族基团或脂族烃基被芳基或基团，R 4是脂族烃基，芳基或脂族烃基，其被芳族基团或基团和/或通过氧或硫原子直接被芳族基团或脂族烃基取代直接由芳族基团取代。这些化合物在药物组合物中是有用的，特别是在抑制血栓素活性的情况下。

6. 发明授权

US4458091A Prostaglandins 失效
公开(公告)号：US4458091A
公开(公告)日：1984-07-03
申请号：US431558
申请日：1982-09-30
申请人： Robert L. Jones , Norman H. Wilson
发明人： Robert L. Jones , Norman H. Wilson
IPC分类号： B29C47/04 , A61K31/19 , A61K31/557 , A61P7/02 , A61P11/00 , B65D33/25 , C07C41/48 , C07C43/315 , C07C45/44 , C07C59/11 , C07C59/13 , C07C59/147 , C07C59/205 , C07C59/31 , C07C59/325 , C07C59/46 , C07C59/54 , C07C59/62 , C07C59/74 , C07C59/80 , C07C59/86 , C07C67/00 , C07C69/608 , C07C69/675 , C07C69/716 , C07C69/732 , C07C69/738 , C07C231/00 , C07C233/08 , C07C235/30 , C07C235/78 , C07C251/42 , C07C251/50 , C07C251/52 , C07C251/54 , C07C253/00 , C07C255/31 , C07C301/00 , C07C311/51 , C07C323/12 , C07C405/00 , C07D213/63 , C07D307/60 , C07D307/93 , C07C57/26
CPC分类号： C07C255/00 , C07C405/0091 , C07C41/48 , C07C43/315 , C07C45/44 , C07C59/13 , C07C59/147 , C07C59/31 , C07C59/325 , C07C59/46 , C07C59/54 , C07C59/62 , C07C59/74 , C07C59/80 , C07C59/86 , C07D307/60 , C07D307/93 , C07B2200/07 , C07C2102/42 , Y10S514/826
摘要： Novel bicyclo [2,2,1] heptanes and hept-2Z-enes are substituted at the 5-position by a 6-carboxyhex-2-enyl group or a modification thereof, and at the 6-position by an aldoxime or ketoxime group which is O-substituted by an aliphatic hydrocarbon residue, an aromatic residue, or an aliphatic hydrocarbon residue substituted directly or through an oxygen or sulphur atom by an aromatic residue. Such compounds may be prepared by the action of an oximating agent on an intermediate which is substituted at the 6-position by an aldehydic or ketonic carbonyl group. The compounds are of value for use in pharmaceutical compositions particularly in the context of the inhibition of thromboxane activity.

8. 发明授权

US5006539A Prostaglandins 失效
标题翻译：前列腺素
公开(公告)号：US5006539A
公开(公告)日：1991-04-09
申请号：US319052
申请日：1989-03-06
申请人： Robert L. Jones , Norman H. Wilson
发明人： Robert L. Jones , Norman H. Wilson
IPC分类号： C07C59/74 , A61K31/16 , A61K31/17 , A61K31/195 , A61K31/215 , A61K31/557 , A61P7/02 , A61P11/08 , A61P29/00 , C07C43/315 , C07C45/44 , C07C51/00 , C07C59/325 , C07C59/353 , C07C59/62 , C07C59/80 , C07C59/86 , C07C67/00 , C07C69/608 , C07C69/716 , C07C69/738 , C07C229/28 , C07C229/32 , C07C231/00 , C07C233/05 , C07C233/65 , C07C235/06 , C07C235/20 , C07C235/46 , C07C237/24 , C07C239/00 , C07C275/26 , C07C275/28 , C07C335/16 , C07C401/00 , C07C405/00 , C07D213/55 , C07D277/62 , C07D307/00 , C07D493/00 , C07D493/08
CPC分类号： C07D493/08 , C07C255/00 , C07C405/0041 , C07C405/0091 , C07C43/315 , C07C45/44 , C07C59/62
摘要： Novel compounds have a formula (I) ##STR1## wherein ##STR2## represents a bicyclo [2,2,1] hept-2Z-ene, bicyclo [2,2,1]heptane, 7-oxa-bicyclo [2,2,1] hept-2Z-ene, 7-oxa-bicyclo [2,2,1] heptane, bicyclo [2,2,2] oct-2Z-ene or bicyclo [2,2,2] octane substituted at the 5-position by the group R.sup.1 and at the 6-position by the group ANR.sup.2 R, a 6,6-dimethyl-bicyclo [3,1,1] heptane substituted at the 2-position by the group R.sup.1 and at the 3-position by the group ANR.sup.2 R or at the 2-position by the group ANR.sup.2 R and at the 3-position by the group R.sup.1, a cyclohex-1-ene or cyclohexane substituted at the 4-position by the group R.sup.1 and at the 5-position by the group ANR.sup.2 R or a 1-hydroxyclopentane substituted at the 2-position by the group R.sup.1 and at the 2-position by the group ANR.sup.2 R, R.sup.1 is a 6-carboxyhex-2-enyl group or a modification thereof as defined herein; A is an unbranched or branched aliphatic hydrocarbon group with a chain length between the points of attachment to the divalent cyclic group and to the group NR.sup.2 R of 1 to 5 carbon atoms or such a group substituted by an aromatic group; R.sup.2 is hydrogen, an aliphatic hydrocarbon group, an aromatic group or an aliphatic hydrocarbon group substituted by an aromatic group or groups; and R is a group --CO.NR.sup.3 R.sup.4, --CS.NR.sup.3 R.sup.4, --CNH.NR.sup.3 R.sup.4, --CO.R.sup.4 or --CO.R.sup.4 in which R.sup.3 is hydrogen, an aliphatic hydrocarbon group, an aromatic group or an aliphatic hydrocarbon group substituted by an aromatic group or groups, and R.sup.4 is an aliphatic hydrocarbon group, an aromatic group or an aliphatic hydrocarbon group substituted directly by an aromatic group or groups and/or through an oxygen or sulphur atom either by an aromatic group or by an aliphatic hydrocarbon group substituted directly by an aromatic group or groups. The compounds are of value for use in pharmaceutical compositions particularly in the context of the inhibition of thromboxane activity.

9. 发明授权

US4628061A Prostaglandins 失效
公开(公告)号：US4628061A
公开(公告)日：1986-12-09
申请号：US531899
申请日：1983-08-23
申请人： Robert L. Jones , Norman H. Wilson
发明人： Robert L. Jones , Norman H. Wilson
IPC分类号： C07C59/74 , A61K31/16 , A61K31/17 , A61K31/195 , A61K31/215 , A61K31/557 , A61P7/02 , A61P11/08 , A61P29/00 , C07C43/315 , C07C45/44 , C07C51/00 , C07C59/325 , C07C59/353 , C07C59/62 , C07C59/80 , C07C59/86 , C07C67/00 , C07C69/608 , C07C69/716 , C07C69/738 , C07C229/28 , C07C229/32 , C07C231/00 , C07C233/05 , C07C233/65 , C07C235/06 , C07C235/20 , C07C235/46 , C07C237/24 , C07C239/00 , C07C275/26 , C07C275/28 , C07C335/16 , C07C401/00 , C07C405/00 , C07D213/55 , C07D277/62 , C07D307/00 , C07D493/00 , C07D493/08 , A61K31/34 , C07C177/00
CPC分类号： C07D493/08 , C07C255/00 , C07C405/0041 , C07C405/0091 , C07C43/315 , C07C45/44 , C07C59/62
摘要： Novel compounds have a formula (I) ##STR1## wherein ##STR2## represents a bicyclo [2,2,1] hept-2Z-ene, bicyclo [2,2,1] heptane, 7-oxa-bicyclo [2,2,1] hept-2Z-ene, 7-oxa-bicyclo [2,2,1] heptane, bicyclo [2,2,2] oct-2Z-ene or bicyclo [2,2,2] octane substituted at the 5-position by the group R.sup.1 and at the 6-position by the group ANR.sup.2 R, a 6,6-dimethyl-bicyclo [3,1,1] heptane substituted at the 2-position by the group R.sup.1 and at the 3-position by the group ANR.sup.2 R or at the 2-position by the group ANR.sup.2 R and at the 3-position by the group R.sup.1, a cyclohex-1-ene or cyclohexane substituted at the 4-position by the group R.sup.1 and at the 5-position by the group ANR.sup.2 R or a 1-hydroxycyclopentane substituted at the 2-position by the group R.sup.1 and at the 2-position by the group ANR.sup.2 R, R.sup.1 is a 6-carboxyhex-2-enyl group or a modification thereof as defined herein; A is an unbranched or branched aliphatic hydrocarbon group with a chain length between the points of attachment to the divalent cyclic group and to the group NR.sup.2 R of 1 to 5 carbon atoms or such a group substituted by an aromatic group; R.sup.2 is hydrogen, an aliphatic hydrocarbon group, an aromatic group or an aliphatic hydrocarbon group substituted by an aromatic group or groups; and R is a group --CO.NR.sup.3 R.sup.4, --CS.NR.sup.3 R.sup.4, --CNH.NR.sup.3 R.sup.4, --CO.R.sup.4 or --CS.R.sup.4 in which R.sup.3 is hydrogen, an aliphatic hydrocarbon group, an aromatic group or an aliphatic hydrocarbon group substituted by an aromatic group or groups, and R.sup.4 is an aliphatic hydrocarbon group, an aromatic group or an aliphatic hydrocarbon group substituted directly by an aromatic group or groups and/or through an oxygen or sulphur atom either by an aromatic group or by an aliphatic hydrocarbon group substituted directly by an aromatic group or groups. The compounds are of value for use in pharmaceutical compositions particularly in the context of the inhibition of thromboxane activity.

10. 发明授权

US4438136A Prostaglandins 失效
标题翻译：前列腺素
公开(公告)号：US4438136A
公开(公告)日：1984-03-20
申请号：US419206
申请日：1982-09-17
申请人： Robert L. Jones , Norman H. Wilson
发明人： Robert L. Jones , Norman H. Wilson
IPC分类号： A61K31/19 , A61K31/557 , A61P7/02 , A61P43/00 , C07C41/54 , C07C43/315 , C07C45/44 , C07C59/46 , C07C59/62 , C07C59/74 , C07C59/80 , C07C67/00 , C07C239/00 , C07C241/00 , C07C251/82 , C07C281/08 , C07C405/00 , A61K31/24
CPC分类号： C07C251/72 , C07C405/0091 , C07C41/48 , C07C45/44 , C07C59/46 , C07C59/62 , C07C59/74 , C07C59/80 , C07C2102/42 , Y10S514/826 , Y10S514/889
摘要： Novel bicyclo [2,2,1] heptanes and hept-2-enes are substituted at the 5-position by a 6-carboxyhex-2-enyl group or a modification thereof, and at the 6-position by a grouping --C(R).dbd.N--NHCO--(NH).sub.a --R' in which R is hydrogen, an aliphatic hydrocarbon residue, an aromatic residue or an aliphatic hydrocarbon residue substituted by an aromatic residue, a is 0 or 1 and R' is an aliphatic hydrocarbon residue, an aromatic residue, or an aliphatic hydrocarbon residue substituted directly or through an oxygen or sulphur atom by an aromatic residue. The compounds are of value for use in pharmaceutical compositions particularly in the context of the inhibition of thromboxane activity.
摘要翻译：新的双环[2,2,1]庚烷和庚-2-烯在5-位被6-羧基己-2-烯基或其修饰取代，并且在6位被-C（ R）= N-NHCO-（NH）aR'，其中R是氢，脂族烃残基，芳族残基或被芳族残基取代的脂族烃残基，a是0或1，R'是脂族烃残基芳族残基，或直接或通过芳族残基被氧或硫原子取代的脂族烃残基。这些化合物在药物组合物中是有用的，特别是在抑制血栓素活性的情况下。

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