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1. 发明授权

US4973704A Pyrrolyl intermediates in the synthesis of pyrrole analogs of mevalonolactone and derivatives thereof 失效
公开(公告)号：US4973704A
公开(公告)日：1990-11-27
申请号：US338909
申请日：1989-04-14
申请人： James R. Wareing
发明人： James R. Wareing
IPC分类号： C07D207/32 , C07D207/337 , C07D307/54 , C07D333/24
CPC分类号： C07D207/337 , C07D307/54 , C07D333/24
摘要： Compounds of the formula ##STR1## wherein R.sub.1 is C.sub.1-6 alkyl not containing an asymmetric carbon atom, C.sub.3-7 cycloalkyl or ##STR2## wherein R.sub.5, R.sub.6 and R.sub.7 are as defined below, R.sub.2 is C.sub.1-6 alkyl not containing an asymmetric carbon atom, C.sub.3-7 cycloalkyl or ##STR3## wherein R.sub.8, R.sub.9 and R.sub.10 are as defined below, R.sub.3 is hydrogen, C.sub.1-6 alkyl not containing an asymmetric carbon atom, C.sub.3-7 cycloalkyl or ##STR4## wherein R.sub.11, R.sub.12 and R.sub.13 are as defined below, R.sub.4 is hydrogen, C.sub.1-6 alkyl not containing an asymmetric carbon atom, C.sub.3-7 cycloalkyl or ##STR5## wherein R.sub.14, R.sub.15 and R.sub.16 are as defined below, X is --(CH.sub.2).sub.m --, --CH.dbd.CH--, --CH.dbd.CH--CH.sub.2 --or --CH.sub.2 --CH.dbd.CH--, wherein m is 0, 1, 2 or 3, andZ is ##STR6## wherein R.sub.17 is hydrogen or C.sub.1-3 alkyl, andR.sub.18 is hydrogen, R.sub.19 or M, whereinR.sub.19 is a physiologically acceptable ester group, andM is a pharmaceutically acceptable cation,whereineach of R.sub.5, R.sub.8, R.sub.11 and R.sub.14 is independently hydrogen, C.sub.1-3 alkyl, n-butyl, i-butyl, t-butyl, C.sub.1-3 alkoxy, n-butoxy, i-butoxy, trifluoromethyl, fluoro, chloro, bromo, phenyl, phenoxy or benzyloxy,each of R.sub.6, R.sub.9, R.sub.12 and R.sub.15 is independently hydrogen, C.sub.1-3 alkyl, C.sub.1-3 alkoxy, trifluoromethyl, fluoro, chloro, bromo, phenoxy or benzyloxy, andeach of R.sub.7, R.sub.10, R.sub.13 and R.sub.16 is independently hydrogen, C.sub.1-2 alkyl, C.sub.1-2 alkoxy, fluoro or chloro,with the provisos that not more than one substituent on each of Rings A, B, C and D independently is trifluoromethyl, not more than one substituent on each of Rings A, B, C and D independently is phenoxy, and not more than one substituent on each of Rings A, B, C and D independently is benzyloxy,with the provisos that (i) the -X-Z group is in the 2- or 3-position of the pyrrole ring, (ii) the -X-Z group is ortho to both R.sub.1 and R.sub.2 and (iii) R.sub.3 is ortho to R.sub.2, the use thereof for inhibiting cholesterol biosynthesis and lowering the blood cholesterol level and, therefore, in the treatment of hyperlipoproteinemia and atherosclerosis, pharmaceutical compositions comprising such compounds and processes for and intermediates in the synthesis of such compounds.

2. 发明授权

US4677211A Preparation of lactones 失效
标题翻译：内酯的制备
公开(公告)号：US4677211A
公开(公告)日：1987-06-30
申请号：US759537
申请日：1985-07-26
申请人： Charles F. Jewell, Jr. , James R. Wareing
发明人： Charles F. Jewell, Jr. , James R. Wareing
IPC分类号： C07F3/14 , C07F7/18 , C07F7/08 , C07C69/76
CPC分类号： C07F7/1852 , C07F3/14 , C07F7/1856
摘要： 7-Substituted lower alkyl hept-6-enoates and 4-hydroxytetrahydropyran-2-ones bearing 6-olefinic substituents (e.g.,) ethyl erythro-3,5-dihydroxy-7-phenyl-hept-6-enoates are prepared by a multi-step process. The process involves 3-protected-lower alkyl 3,5-dihydroxy-hept-6-enoates, which are obtained by cleaving corresponding 6.alpha.-vinyl-4.beta.-protected hydroxy-tetrahydro 2H-pyran-2-ones. The final products are useful as anti hypercholesteremic agents.
摘要翻译： 7-取代的低级烷基庚-6-烯酸酯和含有6-烯烃取代基的4-羟基四氢吡喃-2-酮（例如），赤型-3,5-二羟基-7-苯基 - 庚-6-烯酸乙酯通过多步骤过程该方法包括通过裂解相应的6个α-乙烯基-4β-保护的羟基 - 四氢-2H-吡喃-2-酮的3-保护的低级烷基3,5-二羟基 - 庚-6-烯酸酯。最终产品可用作抗高胆固醇剂。

3. 发明授权

US4474971A (Tetrahydropyran-2-yl)-aldehydes 失效
标题翻译：（四氢吡喃-2-基） - 醛
公开(公告)号：US4474971A
公开(公告)日：1984-10-02
申请号：US427605
申请日：1982-09-29
申请人： James R. Wareing
发明人： James R. Wareing
IPC分类号： C07D309/10 , C07D309/30 , C07D493/04 , C07F7/18 , C07H15/04 , C07H23/00 , C07D309/06
CPC分类号： C07D493/04 , C07D309/10 , C07D309/30 , C07F7/1856 , C07H15/04 , C07H23/00
摘要： Single enanitiomers of 6-(2-hydrocarbyl-substituted ethenyl)-bearing, 4-hydroxy tetrahydro-2H-pyran-2-ones, e.g., 6.alpha.-[2-(2-methyl-1-naphthyl)ethenyl]-3,4,5,6-tetrahydro-4.beta.-hydroxy-2H-pyran-2-one (4R,6S) are obtained by a multi-step process which includes protecting and deprotecting hydroxy groups at various stages.
摘要翻译： 6-（2-烃基取代的乙烯基） - 核 - 4-羟基四氢-2H-吡喃-2-酮的单烯基单体，例如6α-[2-（2-甲基-1-萘基）乙烯基] -3 ，4,5,6-四氢-4β-羟基-2H-吡喃-2-酮（4R，6S）通过多步法制备，其包括在各个阶段保护和脱保护羟基。

4. 发明授权

US4851427A Pyrrole analogs of mevalonolactone, derivatives thereof and pharmaceutical use 失效
公开(公告)号：US4851427A
公开(公告)日：1989-07-25
申请号：US919275
申请日：1986-10-15
申请人： James R. Wareing
发明人： James R. Wareing
IPC分类号： C07D207/32 , C07D207/337 , C07D307/54 , C07D333/24
CPC分类号： C07D207/337 , C07D307/54 , C07D333/24
摘要： Compounds of the formula ##STR1## wherein R.sub.1 is C.sub.1-6 alkyl not containing an asymmetric carbon atom, C.sub.3-7 cycloalkyl or ##STR2## wherein R.sub.5, R.sub.6 and R.sub.7 are as defined below, R.sub.2 is C.sub.1-6 alkyl not containing an asymmetric carbon atom, C.sub.3-7 cycloalkyl or ##STR3## wherein R.sub.8, R.sub.9 and R.sub.10 are as defined below. R.sub.3 is hydrogen, C.sub.1-6 alkyl not containing an asymmetric carbon atom, C.sub.3-7 cycloalkyl or ##STR4## wherein R.sub.11, R.sub.12 and R.sub.13 are as defined below, R.sub.4 is hydrogen, C.sub.1-6 alkyl not containing an asymmetric carbon atom, C.sub.7-7 cycloalkyl or ##STR5## wherein R.sub.14, R.sub.15 and R.sub.16 are as defined below, X is --(CH.sub.2).sub.m --, --CH.dbd.CH--, --CH.dbd.CH--CH.sub.2 -- or --CH.sub.2 --CH.dbd.CH--, wherein m is 0, 1, 2 or 3, andZ is ##STR6## wherein R.sub.17 is hydrogen or C.sub.1-3 alkyl, and R.sub.18 is hydrogen, R.sub.19 or M, wherein R.sub.19 is a physiologically acceptable ester group, andM is a pharmaceutically acceptable cation, wherein each of R.sub.5, R.sub.8, R.sub.11 and R.sub.14 is independently hydrogen, C.sub.1-3 alkyl, n-butyl, i-butyl, t-butyl, C.sub.1-3 alkoxy, n-butoxy, i-butoxy, trifluoromethyl, fluoro, chloro, bromo, phenyl, phenoxy or benzyloxy, each of R.sub.6, R.sub.9, R.sub.12 and R.sub.15 is independently hydrogen, C.sub.1-3 alkyl, C.sub.1-3 alkoxy, trifluoromethyl, fluoro, chloro, bromo, phenoxy or benzyloxy, and each of R.sub.7, R.sub.10, R.sub.13 and R.sub.16 is independently hydrogen, C.sub.1-2 alkyl, C.sub.1-2 alkoxy, fluoro or chloro, with the provisos that not more than one substituent on each of Rings A, B, C and D independently is trifluoromethyl, not more than one substituent on each of Rings A, B, C and D independently is phenoxy, and not more than one substituent on each of Rings A, B, C and D independently is benzyloxy,with the provisos that (i) the --X--Z group is in the 2- or 3-position of the pyrrole ring, (ii) the --X--Z group is ortho to both R.sub.1 and R.sub.2, and (iii) R.sub.3 is ortho to R.sub.2, the use thereof for inhibiting cholesterol biosynthesis and lowering the blood cholesterol level and, therefore, in the treatment of hyperlipoproteinemia and atherosclerosis, pharmaceutical compositions comprising such compounds and processes for and intermediates in the synthesis of such compounds.

5. 发明授权

US4808607A Imidazole analogs of mevalonolactone and derivatives thereof for use in inhibiting cholesterol biosynthesis and lowering blood cholesterol level 失效
标题翻译：用于抑制胆固醇生物合成和降低血液胆固醇水平的甲羟戊酸内酯及其衍生物的咪唑类似物
公开(公告)号：US4808607A
公开(公告)日：1989-02-28
申请号：US123511
申请日：1987-11-20
申请人： James R. Wareing
发明人： James R. Wareing
IPC分类号： C07D233/54 , C07D233/64 , C07F7/18 , C07F9/6506 , A61K31/415
CPC分类号： C07D233/64 , C07F7/1852 , C07F7/1856 , C07F9/65062
摘要： Compounds of the formula ##STR1## and the pharmaceutically acceptable acid addition salts thereof, wherein the various substituents are defined hereinbelow and the use thereof for inhibiting cholesterol biosynthesis and lowering the blood cholesterol level and, therefore, in the treatment of hyperlipoproteinemia and atherosclerosis, pharmaceutical compositions comprising such compounds and processes for and intermediates in the synthesis of such compounds.
摘要翻译：式“IMAGE”的化合物及其药学上可接受的酸加成盐，其中各种取代基在下文中定义，以及其用于抑制胆固醇生物合成和降低血液胆固醇水平的用途，因此在治疗高脂蛋白血症和动脉粥样硬化时，药物包含这些化合物的组合物和合成这些化合物的方法和中间体。

6. 发明授权

US4668794A Intermediate imidazole acrolein analogs 失效
标题翻译：中间体咪唑丙烯醛类似物
公开(公告)号：US4668794A
公开(公告)日：1987-05-26
申请号：US736679
申请日：1985-05-22
申请人： James R. Wareing
发明人： James R. Wareing
IPC分类号： C07D233/54 , C07D233/64 , C07D405/00 , C07F7/18 , C07F9/54 , C07F9/6506
CPC分类号： C07D233/64 , C07F7/1852 , C07F7/1856 , C07F9/65062
摘要： Compounds of the formula ##STR1## and the pharmaceutically acceptable acid addition salts thereof, wherein the various substituents are defined hereinbelow, the use thereof for inhibiting cholesterol biosynthesis and lowering the blood cholesterol level and, therefore, in the treatment of hyperlipoproteinemia and atherosclerosis, pharmaceutical compositions comprising such compounds and processes for and intermediates in the synthesis of such compounds.
摘要翻译：式IMA的化合物及其药学上可接受的酸加成盐，其中各种取代基在下文中定义，其用于抑制胆固醇生物合成和降低血液胆固醇水平，因此用于治疗高脂蛋白血症和动脉粥样硬化，药物包含这些化合物的组合物和合成这些化合物的方法和中间体。

7. 发明授权

US4650890A Preparation of olefinic compounds and intermediates thereof 失效
标题翻译：烯烃化合物的制备及其中间体
公开(公告)号：US4650890A
公开(公告)日：1987-03-17
申请号：US759536
申请日：1985-07-26
申请人： Charles F. Jewell, Jr. , James R. Wareing
发明人： Charles F. Jewell, Jr. , James R. Wareing
IPC分类号： C07D209/24 , C07D309/30 , C07F7/18 , C07B41/06 , C07C69/738 , C07C69/732 , C07C67/313
CPC分类号： C07D309/30 , C07D209/24 , C07F7/1852
摘要： 7-Substituted lower alkyl hept-6-enoates and 4-hydroxy-tetrahydropyran-2-ones bearing 6-olefinic substituents (E), (Z), ethyl erythro-3,5-dihydroxy-7-phenyl-hept-6-enates are prepared by a multi-step process involving lower alkyl 3,5-dihydroxy-hept-6-enates. The final products are useful as anti hypercholesteremic agents.
摘要翻译： 7-取代的低级烷基庚-6-烯酸酯和含有6-烯烃取代基（E），（Z），乙基赤 - 3,5-二羟基-7-苯基 - 庚-6-烯的4-羟基 - 四氢吡喃-2-酮烯化物通过涉及3,5-二羟基 - 庚-6-烯酸低级烷基酯的多步法制备。最终产品可用作抗高胆固醇剂。

8. 发明授权

US4625039A 4-trisubstituted silyl protected hydroxy-6-oxo-tetrahydropyran-2-yl-aldehyde intermediates 失效
标题翻译： 4-三取代甲硅烷基保护的羟基-6-氧代 - 四氢吡喃-2-基 - 醛中间体
公开(公告)号：US4625039A
公开(公告)日：1986-11-25
申请号：US563945
申请日：1983-12-21
申请人： Charles F. Jewell, Jr. , James R. Wareing
发明人： Charles F. Jewell, Jr. , James R. Wareing
IPC分类号： C07D405/06 , C07F7/18 , C07D309/30
CPC分类号： C07D405/06 , C07F7/1856 , Y02P20/55
摘要： 6-trans-indol-2-yl-ethenyl)-4-hydroxy-tetrahydro-2H-pyran-2-ones of formula I are obtained by a multi-step reaction involving the procedure: ##STR1## wherein p.sup.1 is trisubstituted silyl protective group, and Z is a 2-indolyl radical which may be bear at the 4, 5, 6 and 7-positions up to two substituents such as alkyl, alkoxy, halo and CF.sub.3, and at either one the 1 or 3-positions a substituted or unsubstituted phenyl; and at the other an assymetric alkyl, cycloalkyl or aralkyl radical. Compounds I, e.g. (E)-trans-6-[1'-methyl-3'-(4"-fluorophenyl)indol-2'-ylethenyl]3,4,5,6-tetrahydro-4-hydroxy-2H-pyran-2-one(4R,6S); are useful as anti-atheroselerotic agents.
摘要翻译： 6-反式 - 吲哚-2-基 - 乙烯基）-4-羟基 - 四氢-2H-吡喃-2-酮通过涉及以下步骤的多步反应获得：其中p1为三取代甲硅烷基保护基，Z是可以在至多两个取代基例如烷基，烷氧基，卤素和CF 3的4,5,6和7位上具有的2-吲哚基，并且在1或3 - 取代或未取代的苯基; 而另一个是不对称的烷基，环烷基或芳烷基。化合物I，例如（E） - 反式-6- [1'-甲基-3' - （4“ - 氟苯基）吲哚-2'-基乙烯基] 3,4,5,6-四氢-4-羟基-2H-吡喃-2 （4R，6S）; 作为抗动脉粥样硬化剂有用。

9. 发明授权

US4927851A Analogs of mevalonolactone and derivatives thereof 失效
标题翻译：甲羟戊酸内酯及其衍生物的类似物
公开(公告)号：US4927851A
公开(公告)日：1990-05-22
申请号：US242667
申请日：1988-09-12
申请人： Robert E. Damon, II , James R. Wareing
发明人： Robert E. Damon, II , James R. Wareing
IPC分类号： C07D207/32 , C07D207/337 , C07D307/54 , C07D333/24
CPC分类号： C07D207/337 , C07D307/54 , C07D333/24
摘要： Compounds of the formula ##STR1## in which Y is ##STR2## X is O or S; Z is --CHOH--CH.sub.2 --CHOH--CH.sub.2 --COOH, an ester or salt thereof or the lactone thereof; andeach of R.sup.1 R.sup.2 and R.sup.3 can be alkyl, cycloalkyl; or substituted or unsubstituted phenyl; and additionally R.sup.3 can be hydrogen, are obtained by a multi-step process and are useful in the treatment of atherosclerosis, e.g. sodium (E)-7-(4-phenyl-2-isopropyl-5-phenylthien-3-yl)-3,5-dihydroxyhept-6-enoate.
摘要翻译：其中Y是X或X的式“IMAGE”的化合物是O或S; Z是-CHOH-CH 2 -CHOH-CH 2 -COOH，其酯或其盐或其内酯; R1 + L，R2和R3各自可以是烷基，环烷基，或取代或未取代的苯基; 另外R3可以是氢，通过多步法获得并且可用于治疗动脉粥样硬化，例如，（E）-7-（4-苯基-2-异丙基-5-苯基噻吩-3-基）-3,5-二羟基庚-6-烯酸钠。

10. 发明授权

US4829081A Analogs of mevalonolactone and derivatives thereof 失效
标题翻译：甲羟戊酸内酯及其衍生物的类似物
公开(公告)号：US4829081A
公开(公告)日：1989-05-09
申请号：US945428
申请日：1986-12-22
申请人： Robert E. Damon, II , James R. Wareing
发明人： Robert E. Damon, II , James R. Wareing
IPC分类号： C07D207/32 , C07D207/337 , C07D307/54 , C07D333/24
CPC分类号： C07D207/337 , C07D307/54 , C07D333/24
摘要： Compounds of the formula ##STR1## in which Y is ##STR2## X is O or S; Z is --CHOH--CH.sub.2 --CHOH--CH.sub.2 --COOH, an ester or salt thereof or the lactone thereof; andeach of R.sup.1, R.sup.2 and R.sup.3 can be alkyl, cycloalkyl; or substituted or unsubstituted phenyl; and additionally R.sup.3 can be hydrogen, are obtained by a multi-step process and are useful in the treatment of atherosclerosis, e.g. sodium(E)-7-(4-phenyl-2-isopropyl-5-phenylthien-3-yl)-3,5-dihydroxyhept-6- enoate.
摘要翻译：其中Y是X或X的式“IMAGE”的化合物是O或S; Z是-CHOH-CH 2 -CHOH-CH 2 -COOH，其酯或其盐或其内酯; R 1，R 2和R 3可以是烷基，环烷基，或取代或未取代的苯基; 另外R3可以是氢，通过多步法获得并且可用于治疗动脉粥样硬化，例如，（E）-7-（4-苯基-2-异丙基-5-苯基噻吩-3-基）-3,5-二羟基庚-6-酯的钠盐。

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