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1. 发明授权

US5030632A Low dose temazepam 失效
标题翻译：低剂量替马西泮
公开(公告)号：US5030632A
公开(公告)日：1991-07-09
申请号：US569787
申请日：1990-08-17
申请人： William R. Sterling
发明人： William R. Sterling
IPC分类号： A61K9/48 , A61K31/55 , C07D243/24
CPC分类号： A61K9/48 , A61K31/55 , C07D243/24 , Y10S514/923 , Y10S514/962
摘要： This invention relates to a hard gelatin capsule containing no more than 5 to 10 milligrams of crystalline temazepam and its use in the treatment of transient insomnia.
摘要翻译：本发明涉及含有不超过5至10毫克结晶的替马西平的硬明胶胶囊及其在治疗短暂性失眠中的用途。

2. 发明授权

US5001255A Idene analogs of mevalonolactone and derivatives thereof 失效
标题翻译：甲羟戊酸内酯类似物及其衍生物
公开(公告)号：US5001255A
公开(公告)日：1991-03-19
申请号：US214560
申请日：1988-07-01
申请人： Faizulla G. Kathawala , Sompong Wattanasin
发明人： Faizulla G. Kathawala , Sompong Wattanasin
IPC分类号： C07C17/26 , C07C45/00 , C07C47/24 , C07C47/57 , C07D309/30
CPC分类号： C07D309/30 , C07C17/2632 , C07C45/00 , C07C47/24 , C07C47/57
摘要： Compounds of the formula ##STR1## 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：下式的化合物其用于抑制胆固醇生物合成和降低血液胆固醇水平以及因此在治疗高脂蛋白血症和动脉粥样硬化中的用途，包含这些化合物的药物组合物及其合成方法和中间体。

3. 发明授权

US4939159A Azaindole derivatives useful as cholesterol biosynthesis inhibitors 失效
标题翻译：可用作胆固醇生物合成抑制剂的Azaindole衍生物
公开(公告)号：US4939159A
公开(公告)日：1990-07-03
申请号：US320664
申请日：1989-03-08
申请人： Paul L. Anderson , Faizulla G. Kathawala , Nicholas A. Paolella , Sompong Wattanasin
发明人： Paul L. Anderson , Faizulla G. Kathawala , Nicholas A. Paolella , Sompong Wattanasin
IPC分类号： C07D471/04
CPC分类号： C07D471/04
摘要： Compounds of the formula I: ##STR1## wherein X is the residue of an unsubstituted 6-membered aromatic ring having 3 carbon atoms and one nitrogen atom;R.sup.1 is C.sub.1-6 primary alkyl (free of asymmetric carbon atoms), or isopropyl;R.sup.2 is substituted or unsubstituted phenyl, primary or secondary C.sub.1-6 alkyl (free of asymmetric carbons),C.sub.3-6 cycloalkyl or phenalkyl as defined in the Specification ##STR2## in which R.sup.8 is hydrogen, R.sup.9 or M, whereinR.sup.9 is a physiologically acceptable and hydrolyzable ester group, andM is a pharmaceutically acceptable cation;are obtained by multi-step processes and are useful as cholesterol biosynthesis inhibitors. 3
摘要翻译：式I的化合物：其中X是具有3个碳原子和一个氮原子的未取代的6元芳环的残基; R1是C1-6的伯烷基（不含不对称碳原子）或异丙基; R2是取代或未取代的苯基，主要或仲C 1-6烷基（不含不对称碳），如说明书中所定义的C 3-6环烷基或苯烷基，其中R 8是氢，R 9或M 其中R9是生理上可接受和可水解的酯基，M是药学上可接受的阳离子; 通过多步法获得并且可用作胆固醇生物合成抑制剂。

4. 发明授权

US4892879A 1-substituted-4-(thiazolyl-2-)-piperazines, -piperidines and tetrahydro-pyridines useful as anxioltic, psychogeriatric, antisepressant and antischiziphrenic agents 失效
标题翻译： 1-取代-4-（噻唑基-2-） - 哌嗪类，哌啶类和四氢吡啶类，可用作抗焦虑药，精神病药，抗抑郁药和抗消痰剂
公开(公告)号：US4892879A
公开(公告)日：1990-01-09
申请号：US151349
申请日：1988-02-02
申请人： Dieter Sorg
发明人： Dieter Sorg
IPC分类号： C07D277/38 , C07D277/42 , C07D417/12 , C07D417/14 , C07D471/04 , C07D513/04
CPC分类号： C07D417/12 , C07D277/42 , C07D417/14 , C07D471/04 , C07D513/04
摘要： Thiazoles or pharmaceutically acceptable acid addition salts thereof are useful as anxiolytic, psychogeriatric, antidepressant and antischizophrenic agents.

5. 发明授权

US4845129A Diaryl substituted cyclopentane and cyclopentene derivatives 失效
标题翻译：二芳基取代的环戊烷和环戊烯衍生物
公开(公告)号：US4845129A
公开(公告)日：1989-07-04
申请号：US167766
申请日：1988-03-14
申请人： Robert C. Anderson , William J. Houlihan , Howard C. Smith , Edwin B. Villhauer
发明人： Robert C. Anderson , William J. Houlihan , Howard C. Smith , Edwin B. Villhauer
IPC分类号： C07C43/21 , C07C43/215 , C07C43/23 , C07C45/30 , C07C45/56 , C07C45/62 , C07C45/66 , C07C45/68 , C07C49/657 , C07C49/683 , C07C49/753 , C07C205/45 , C07C217/74 , C07C251/44
CPC分类号： C07C251/44 , C07C205/45 , C07C217/74 , C07C43/21 , C07C43/215 , C07C43/23 , C07C45/30 , C07C45/567 , C07C45/62 , C07C45/66 , C07C45/68 , C07C49/657 , C07C49/683 , C07C49/753 , C07C2101/08 , C07C2101/10
摘要： The invention discloses certain diaryl substituted cyclopentane and cyclopentene derivatives useful as PAF inhibitors, pharmaceutical compositions containing said compounds as an active ingredient thereof and a method of using such compositions for inhibiting PAF-induced blood platelet aggregation, PAF-mediated broncho-constriction and extravasation, PAF-induced hypotension, PAF-induced ischemic bowel disease and PAF-mediated, endotoxin induced lug injury.
摘要翻译：本发明公开了可用作PAF抑制剂的某些二芳基取代的环戊烷和环戊烯衍生物，含有所述化合物作为其活性成分的药物组合物和使用该组合物抑制PAF诱导的血小板聚集，PAF介导的支气管收缩和外渗的方法， PAF引起的低血压，PAF诱导的缺血性肠病和PAF介导的内毒素引起的耳损伤。

6. 发明授权

US4804679A Erythro-(E)-7-(3'-C1-3alkyl-1'-(3",5"-dimethylphenyl)naphth-2'-yl )-3,5-dihydroxyhept-6-enoic acids and derivatives thereof 失效
标题翻译：（E）-7-（3'-C 1-3烷基-1' - （3“，5” - 二甲基苯基）萘-2'-基）-3,5-二羟基庚-6-烯酸及其衍生物其中
公开(公告)号：US4804679A
公开(公告)日：1989-02-14
申请号：US82873
申请日：1987-08-06
申请人： Paul L. Anderson
发明人： Paul L. Anderson
IPC分类号： A61K31/19 , C07C59/48 , C07D309/30 , A61K31/365
CPC分类号： C07C59/48 , A61K31/19 , C07D309/30
摘要： Compounds of the formula ##STR1## wherein R.sub.1 is C.sub.1-3 alkyl, andZ is ##STR2## wherein R.sub.7 is hydrogen, R.sub.8 or M,whereinR.sub.8 is a physiologically acceptable and hydrolyzable ester group, andM is a pharmaceutically acceptable cation,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：其中R 1是C 1-3烷基，Z是其中R 7是氢，R 8或M，其中R 8是一个生理上可接受和可水解的酯基，M是一个药学上可接受的阳离子，式其用于抑制胆固醇生物合成和降低血液胆固醇水平，并因此降低高脂蛋白血症和动脉粥样硬化的治疗药物，包含这些化合物的药物组合物及其合成方法和中间体。

7. 发明授权

US4992428A 5-aryl-substituted-2,3-dihydro-imidazo[1,2-a]furo- and thieno pyridines 失效
标题翻译： 5-芳基 - 取代-2,3-二氢 - 咪唑并[1,2-a]呋喃和噻吩并吡啶
公开(公告)号：US4992428A
公开(公告)日：1991-02-12
申请号：US363794
申请日：1989-06-09
申请人： William J. Houlihan , Seung H. Cheon
发明人： William J. Houlihan , Seung H. Cheon
IPC分类号： C07D491/14 , C07D491/147 , C07D495/14
CPC分类号： C07D491/14 , C07D495/14
摘要： The invention discloses certain 5-aryl-substituted,2,3-dihydro-imidazo[1,2-a]furo- and thieno pyridines useful as PAF receptor antagonists and for treating tumors, pharmaceutical compositions containing said compounds as an active ingredient thereof and a method of using such compositions for inhibiting PAF-mediated bronchoconstriction and extravasation, for controlling hyperreactive airways, for protecting against endotoxin-induced hypotension and death and for treating tumors.
摘要翻译：本发明公开了可用作PAF受体拮抗剂并用于治疗肿瘤的某些5-芳基取代的2,3-二氢 - 咪唑并[1,2-a]呋喃并噻吩并吡啶，含有所述化合物作为其活性成分的药物组合物和使用这种组合物抑制PAF介导的支气管收缩和外渗，用于控制高反应性气道，用于防止内毒素诱导的低血压和死亡以及用于治疗肿瘤的方法。

8. 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.

9. 发明授权

US4933105A Process for preparation of microspheres 失效
标题翻译：微球制备方法
公开(公告)号：US4933105A
公开(公告)日：1990-06-12
申请号：US193977
申请日：1988-05-13
申请人： Jones W. Fong
发明人： Jones W. Fong
IPC分类号： A61K9/16 , A61K9/50 , B01J13/12
CPC分类号： B01J13/125 , A61K9/1647 , A61K9/1694 , A61K9/50 , Y10S514/951 , Y10S514/963 , Y10S514/965
摘要： Microspheres, prepared by solvent removal from an oil-in-water emulsion using carboxylic acid salt surfactant, e.g., sodium oleate as the emulsifier.
摘要翻译：通过使用羧酸盐表面活性剂例如油酸钠作为乳化剂从水包油乳液中除去溶剂制备的微球。

10. 发明授权

US4870199A Processes for the synthesis of diprotected R[R*,S*]-3,5-dihydroxy-6-oxohexanoate esters 失效
标题翻译：合成二保护R [R *，S *] - 3,5-二羟基-6-氧代己酸酯的方法
公开(公告)号：US4870199A
公开(公告)日：1989-09-26
申请号：US166594
申请日：1988-03-10
申请人： Kau-Ming Chen , Goetz E. Hardtmann , Prasad K. Kapa , George T. Lee , Jerome Linder , Sompong Wattanasin
发明人： Kau-Ming Chen , Goetz E. Hardtmann , Prasad K. Kapa , George T. Lee , Jerome Linder , Sompong Wattanasin
IPC分类号： C07D209/18 , C07D233/54 , C07F7/18
CPC分类号： C07D233/64 , C07D209/18 , C07F7/1852 , Y02P20/55
摘要： Process for the synthesis of compounds of the formula ##STR1## in R[R*,S*] enantiomeric form, wherein each P.sub.1 is independently an hydroxy group-protecting group, andR.sub.2z is C.sub.1-4 alkyl, benzyl or allyl,comprising, as a key step when R.sub.2z is R.sub.2x, the reaction of the compound of the formula ##STR2## in (S) enantiomeric form with a compound of the formulaMg.sup. .circle.+2 (.sup..crclbar. OOC--CH.sub.2 --COOR.sub.2x).sub.2to obtain a compound of the formula ##STR3## in (S) enantiomeric form, and, as a key step when R.sub.2z is R.sub.2y, the reaction of a compound of the formula ##STR4## in (S) enantioimeric form with a compound of the formulaLi.sup..sym..crclbar. CH.sub.2 --COOR.sub.2yto obtain a compound of the formula ##STR5## in (S) enantiomeric form, wherein R.sub.2x is primary or secondary C.sub.1-4 alkyl, benzyl or allyl,R.sub.2y is C.sub.1-4 alkyl not containing an asymmetric carbon atom, andR.sub.3 ' is methyl or ethyl,processes for the synthesis of compounds of the formula ##STR6## comprising reacting a compound of the formula ##STR7## with the reaction product of a strong base and a compound of the formula ##STR8## optionally followed by, when R.sub.2z is allyl, cleavage of the allyl and P.sub.1 groups to obtain the corresponding compound of the formula ##STR9## wherein each R.sub.7 is methyl or ethyl,R is as defined in the specification, and eachP.sub.1 independently and R.sub.2z are as defined above, andthe compounds of the formula ##STR10## wherein R and each R.sub.7 are as defined above.
摘要翻译：用于合成R [R *，S *]对映体形式的式“IMAGE”的化合物的方法，其中每个P1独立地是羟基保护基，R2z是C1-4烷基，苄基或烯丙基，包括作为 R2z为R2x时的关键步骤，式（S）对映异构形式的式（IMA）化合物与式Mg＆cir＆+2（（ - ）OOC-CH2-COOR2x）2的化合物的反应，得到化合物式（S）对映体形式的式（IMAGE）式中，作为R2z为R2y的关键步骤，式（S）对映异构体形式的式“IMAGE”的化合物与式Li ）（ - ）CH2-COOR2y，得到（S）对映异构体形式的下式的化合物，其中R2x是伯或仲C 1-4烷基，苄基或烯丙基，R2y是不含不对称碳原子的C 1-4烷基，并且R 3'是甲基或乙基，用于合成式IMA化合物的方法包括使式IMA的化合物与强碱的反应产物 da化合物，其中当R 2z是烯丙基时，烯丙基和P1基团裂解，得到相应的式“IMAGE”化合物，其中每个R 7是甲基或乙基，R如说明书中所定义，每个P1独立地和R2z如上所定义，并且式“IMAGE”的化合物其中R和每个R 7如上所定义。

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