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1. 发明授权

US5684177A Misoprostol 失效
标题翻译：米索前列醇
公开(公告)号：US5684177A
公开(公告)日：1997-11-04
申请号：US649402
申请日：1996-05-17
申请人： Yee-Fung Lu , Raymond So , Dan To , Casimir G. Antczak
发明人： Yee-Fung Lu , Raymond So , Dan To , Casimir G. Antczak
IPC分类号： C07C405/00 , C07F1/08 , C07F7/22 , C07C177/00
CPC分类号： C07F1/08 , C07C405/00 , C07F7/2212
摘要： In a process for making synthetic prostaglandin-type compounds such as misoprostol, organo metallic cuprate complexes capable of reacting with cyclopentenones are prepared by reaction of an alkyl lithium compound with a cuprous halide, followed by reaction of the resulting complex with a vinyl stannane, using an excess of alkyl lithium in the initial reaction and maintaining the excess present during the formation of the organo metallic cuprate complex.
摘要翻译：在制备合成前列腺素型化合物如米索前列醇的方法中，通过烷基锂化合物与卤化亚铜反应制备能与环戊烯酮反应的有机金属铜酸盐络合物，然后使所得配合物与乙烯基锡烷反应，使用在初始反应中过量的烷基锂，并且在形成有机金属铜酸盐络合物期间保持过量存在。

2. 发明授权

US4820728A Tetraenyl prostaglandins 失效
标题翻译：四烯基前列腺素
公开(公告)号：US4820728A
公开(公告)日：1989-04-11
申请号：US68608
申请日：1987-06-30
申请人： Paul W. Collins , Alan F. Gasiecki
发明人： Paul W. Collins , Alan F. Gasiecki
IPC分类号： C07C405/00 , C07C177/00
CPC分类号： C07C405/00
摘要： This invention encompasses prostaglandins of the formula ##STR1## wherein R represents hydrogen or lower alkyl having 1 to 6 carbon atoms; R.sub.1 represents hydrogen, vinyl, or lower alkyl having 1 to 4 carbon atoms and the wavy line represents R or S stereochemistry; R.sub.2, R.sub.3, and R.sub.4 are hydrogen or lower alkyl having 1 to 4 carbom atoms or R.sub.2 and R.sub.3 together with carbon Y form a cycloalkenyl having 4 to 6 carbon atoms or R.sub.3 and R.sub.4 together with carbons X and Y form a cycloalkenyl having 4 to 6 carbons. Compounds of this invention have potent gastric antisecretory and cytoprotective properties with unexpectedly low diarrheogenic side effects.
摘要翻译：本发明包括式IMA的前列腺素，其中R表示氢或具有1至6个碳原子的低级烷基; R1表示氢，乙烯基或具有1至4个碳原子的低级烷基，波浪线表示R或S立体化学; R 2，R 3和R 4是氢或具有1至4个碳原子的低级烷基或R 2和R 3与碳Y一起形成具有4至6个碳原子的环烯基，或者R 3和R 4与碳一起形成X和Y形成具有4至 6个碳。本发明的化合物具有强烈的胃分泌和细胞保护性能，具有出乎意料的低泻药副作用。

3. 发明授权

US4766147A Novel 5-membered cyclic compounds, process for production thereof, and pharmaceutical use thereof 失效
标题翻译：新的5元环状化合物，其制备方法及其药物用途
公开(公告)号：US4766147A
公开(公告)日：1988-08-23
申请号：US823146
申请日：1986-01-29
申请人： Ryoji Noyori , Masanori Fukushima , Seizi Kurozumi , Satoshi Sugiura
发明人： Ryoji Noyori , Masanori Fukushima , Seizi Kurozumi , Satoshi Sugiura
IPC分类号： C07C59/90 , C07C405/00 , C07F7/18 , C07C177/00 , A61K31/557
CPC分类号： C07C405/00 , C07C405/0025 , C07C59/90 , C07F7/1856
摘要： Novel 5-alkylidene-4-substituted-2-cyclopentenones and 5-(1-hydroxy-aliphatic hydrocarbon)-4-substituted-2-cyclopentenones.These novel cyclopentenones and 5-alkylidene-3-hydroxy-4-substituted cyclopentanones have a pharmaceutical activity for treatment of tumors.
摘要翻译：新的5-亚烷基-4-取代-2-环戊烯酮和5-（1-羟基 - 脂族烃）-4-取代-2-环戊烯酮。这些新的环戊烯酮和5-亚烷基-3-羟基-4-取代的环戊酮具有治疗肿瘤的药物活性。

4. 发明授权

US4730078A Allenic prostacyclins 失效
标题翻译：美容前列环素
公开(公告)号：US4730078A
公开(公告)日：1988-03-08
申请号：US050257
申请日：1987-05-13
申请人： Stevan W. Djuric , Masateru Miyano
发明人： Stevan W. Djuric , Masateru Miyano
IPC分类号： A61K31/557 , A61P7/02 , C07C59/46 , C07C59/54 , C07C59/56 , C07C67/00 , C07C69/732 , C07C313/00 , C07C317/46 , C07C323/55 , C07C323/56 , C07C405/00 , C07C177/00
CPC分类号： C07C405/0083
摘要： The present invention relates to allenic prostacyclin derivatives of the formula: ##STR1## wherein: n is 0, 1, 2R.sup.1 is hydrogen, lower alkyl, lower hydroxyalkyl, or a pharmaceutically acceptable cation;R.sup.2 is hydrogen, lower alkyl, cycloalkyl, heteroalkyl, halogen, aryl, alkylthio, phenylthio, alkylsulfinyl, phenylsulfonyl, or trifluoromethyl,R.sup.3 is a lower alkyl, a cycloalkyl, phenyl, benzyl, a cycloheteroalkyl, a lower alkyl having one to eight carbons substituted with one or more fluorines or containing 1 or 2 unsaturated bonds; and carbon 15 may be in the R or the S configuration, or a mixture of R and S with the proviso that when R.sup.1 is a lower alkyl or lower hydroxyalkyl that carbon 15 is not in the R configuration.These compounds are useful for the treatment of platelet dysfunction and atherosclerosis. Also disclosed is the process for preparing these compounds and their appropriate intermediates.

5. 发明授权

US4713477A Omega cycloalkyl prostaglandins 失效
标题翻译：欧米茄环烷基前列腺素
公开(公告)号：US4713477A
公开(公告)日：1987-12-15
申请号：US798197
申请日：1985-11-14
申请人： Paul W. Collins , Alan F. Gasiecki
发明人： Paul W. Collins , Alan F. Gasiecki
IPC分类号： C07C405/00 , C07C177/00
CPC分类号： C07C405/0025 , C07C405/00
摘要： This invention encompasses prostaglandins of the formula I ##STR1## wherein R represents hydrogen or lower alkyl containing 1 to 6 carbon atoms;X represents --CH.sub.2 --, --CH.dbd.CH--, --C.tbd.C--, --CH.sub.2 --C.tbd.C--, --CH.sub.2 --CH.dbd.CH-- --CH.sub.2 --CH.sub.2 --CH.sub.2, --CH.dbd.CH--CH.sub.2 --, --C.tbd.C--CH.sub.2 --; andR.sub.1 represents cyclopropyl, cyclobutyl, cyclopentyl, 1-methylcyclopropyl or 1-methylcyclobutyl or XR.sub.1 together represent 1-methyl-1-cyclopropylethyl or 1-methyl-1-cyclobutylethyl; and R.sub.2 is lower alkyl having 1 to 4 carbon atoms or vinyl or ethynyl; the wavy line represents optional R or S sterochemistryThese compounds are potent antisecretory agents.
摘要翻译：本发明包括式I的前列腺素，其中R表示氢或含有1至6个碳原子的低级烷基; X表示-CH 2 - ， - CH = CH - ， - C 3BOND C - ， - CH 2 -CH 3 CH-，-CH 2 -CH = CH- -CH 2 -CH 2 -CH 2，-CH = CH-CH 2 - ， - 3OND C-CH2-; R1代表环丙基，环丁基，环戊基，1-甲基环丙基或1-甲基环丁基或XR1一起代表1-甲基-1-环丙基乙基或1-甲基-1-环丁基乙基; 和R2是具有1至4个碳原子的低级烷基或乙烯基或乙炔基; 波浪线代表任选的R或S类固体化学这些化合物是有效的抗分泌剂。

6. 发明授权

US4705806A Prostacyclin analogs 失效
公开(公告)号：US4705806A
公开(公告)日：1987-11-10
申请号：US877253
申请日：1978-02-13
申请人： Douglas R. Morton, Jr.
发明人： Douglas R. Morton, Jr.
IPC分类号： C07C59/46 , A61K31/557 , A61K31/5575 , A61P43/00 , C07C29/09 , C07C45/60 , C07C45/62 , C07C45/64 , C07C45/67 , C07C51/00 , C07C67/00 , C07C69/732 , C07C401/00 , C07C405/00 , C07D257/04 , C07D309/12 , C07D319/06 , C07F7/18 , C07C177/00
CPC分类号： C07D257/04 , C07C29/095 , C07C405/0083 , C07C45/60 , C07C45/62 , C07C45/64 , C07C45/673 , C07D309/12 , C07D319/06 , C07F7/1856 , C07C2103/08
摘要： Prostacyclin (PGI.sub.2) analogs having a 6a-carba feature, for example a compound of the formula ##STR1## said analogs having pharmacological activity. Processes for preparing them and the appropriate intermediates are disclosed.

7. 发明授权

US4698363A Prostacyclin analogues 失效
标题翻译：前列环素类似物
公开(公告)号：US4698363A
公开(公告)日：1987-10-06
申请号：US799796
申请日：1985-11-20
申请人： Terance W. Hart
发明人： Terance W. Hart
IPC分类号： C07C59/46 , A61K31/557 , A61P1/04 , A61P7/02 , A61P9/10 , A61P9/12 , A61P25/00 , C07C51/00 , C07C59/56 , C07C59/62 , C07C59/80 , C07C67/00 , C07C69/732 , C07C69/734 , C07C69/738 , C07C313/00 , C07C323/55 , C07C405/00 , C07C177/00
CPC分类号： C07C405/0083
摘要： Prostaglandin analogues of the formula: ##STR1## (wherein R.sup.1 represents a hydrogen atom or an aliphatic or alicyclic hydrocarbon radical, Y.sup.1 represents a carbonyl or hydroxymethylene group, A.sup.1 represents an alkylene linkage containing 1, 2 or 3 carbon atoms and optionally bearing a methyl or ethyl substituent, R.sup.2 represents a hydrogen atom or a methyl or ethyl group and R.sup.3 represents a hydrogen atom or R.sup.2 and R.sup.3 form an alkylene linkage containing 2 or 3 carbon atoms, optionally bearing a methyl or ethyl substituent, such that the symbols A.sup.1, R.sup.2 and R.sup.3, together with the carbon atoms through which they are connected, may form a cycloalkyl ring of 5, 6, 7 or 8 carbon atoms, optionally bearing one or two methyl or ethyl substituents, or A.sup.1 and R.sup.3, together with the carbon atom through which they are connected, may form a phenylene ring optionally substituted by a halogen atom or by a trifluoromethyl group or by a straight- or branched-chain alkyl or alkoxy group containing from 1 to 6 carbon atoms, A.sup.2 represents a direct bond or a methylene group optionally bearing one or two methyl or ethyl substituents, X.sup.1 represents an ethylene, transvinylene or ethynylene group, Y.sup.2 represents a carbonyl or hydroxymethylene group, and either (i) A.sup.3 represents a straight- or branched-alkylene chain containing from 1 to 5 carbon atoms, Z.sup.1 represents a direct bond or an oxygen or sulphur atom, and R.sup.4 represents a group R.sup.4' which is an aliphatic or alicyclic hydrocarbon radical, or R.sup.4 represents a phenyl group optionally substituted by a halogen atom or by a trifluoromethyl group or by a straight- or branched-chain alkyl or alkoxy group containing from 1 to 6 carbon atoms, or (ii) A.sup.3 and Z.sup.1 both represent direct bonds and R.sup.4 represents a group R.sup.4' as hereinbefore defined) and cyclodextrin clathrates thereof and non-toxic salts thereof possess useful pharmacological properties.
摘要翻译：具有下式的前列腺素类似物：其中R1表示氢原子或脂族或脂环族烃基，Y1表示羰基或羟基亚甲基，A1表示含有1,2或3个碳原子的亚烷基键，并且任选地带有甲基或乙基取代基，R2表示氢原子或甲基或乙基，R3表示氢原子或R2和R3形成含有2或3个碳原子的亚烷基，任选带有甲基或乙基取代基，符号A1 ，R2和R3与它们连接的碳原子一起可以形成5个，6个，7个或8个碳原子的环烷基环，任选带有一个或两个甲基或乙基取代基，或者A1和R3，以及它们连接的碳原子可以形成任选被卤素原子或三氟甲基取代的亚苯基环或通过含有1至6个碳原子的直链或支链烷基或烷氧基碳原子，A2表示直接键或任选带有一个或两个甲基或乙基取代基的亚甲基，X1表示乙烯，亚乙炔基或亚乙炔基，Y2表示羰基或羟亚甲基，（i）A3表示直链，或含有1至5个碳原子的支链亚烷基，Z1表示直接键或氧或硫原子，R4表示作为脂族或脂环族烃基的基团R4'，或R4表示任选被卤素原子或三氟甲基或含有1至6个碳原子的直链或支链烷基或烷氧基，或（ii）A3和Z1都表示直接键，R4表示如上所定义的基团R4' ）及其环糊精包合物及其无毒盐具有有用的药理学性质。

8. 发明授权

US4692464A Novel prostacyclin derivatives and a process for the preparation thereof 失效
公开(公告)号：US4692464A
公开(公告)日：1987-09-08
申请号：US352411
申请日：1982-02-26
申请人： Werner Skuballa , Bernd Raduchel , Helmut Vorbruggen , Gerda Mannesmann , Wolfgang Losert , Jorge Casals
发明人： Werner Skuballa , Bernd Raduchel , Helmut Vorbruggen , Gerda Mannesmann , Wolfgang Losert , Jorge Casals
IPC分类号： C07D309/12 , A61K31/557 , A61K31/5575 , A61K31/5585 , A61P7/02 , A61P25/02 , A61P43/00 , C07C45/59 , C07C45/67 , C07C45/71 , C07C51/00 , C07C51/353 , C07C59/46 , C07C62/32 , C07C67/00 , C07C67/343 , C07C69/732 , C07C401/00 , C07C405/00 , C07D317/72 , C07D319/12 , C07C177/00
CPC分类号： C07D317/72 , A61K31/557 , C07C405/0083 , C07C45/59 , C07C45/673 , C07C45/71 , C07C62/32 , C07D319/12
摘要： Compounds of the formula ##STR1## wherein R.sub.1 is (a) hydrogen, (b) C.sub.1-10 alkyl, (c) C.sub.1-10 alkyl substituted by halogen; C.sub.1-4 alkoxy; C.sub.6-10 aryl; C.sub.6-10 aryl substituted by 1-3 halogen atoms, a phenyl group, 1-3 C.sub.1-4 alkyl groups or a chloromethyl, fluoromethyl, trifluoromethyl, carboxy, hydroxy or C.sub.1-4 alkoxy group; di-C.sub.1-4 -alkylamino; or tri-C.sub.1-4 -alkylammonium, (d) C.sub.4-10 cycloalkyl, (e) C.sub.4-10 cycloalkyl substituted by C.sub.1-4 alkyl, (f) C.sub.6-10 aryl, (g) C.sub.6-10 aryl substituted by 1-3 halogen atoms, a phenyl group 1-3 C.sub.1-4 alkyl groups or a chloromethyl, fluoromethyl, trifluoromethyl, carboxy, hydroxy or C.sub.1-4 alkoxy group, or (h) an aromatic heterocycle of 5 or 6 ring atoms one of which is O, N or S;A is --CH.sub.2 --CH.sub.2 --, trans--CH.dbd.CH-- or --C.tbd.C--;W is hydroxymethylene, RO-methylene, CH.sub.3 or CH.sub.3, ##STR2## wherein OH or OR is in the .alpha.- or .beta.-position and R is an in vivo hydrolyzable and physiologically acceptable ether or acyl group which is conventional for modifying OH groups in prostaglandins;D and E together are a direct bond, orD is C.sub.1-10 alkylene, C.sub.1-10 alkenylene or C.sub.1-10 alkynylene or one of these groups substituted by fluorine, andE is oxygen, --C.tbd.C-- or a direct bond;R.sub.2 is (a) a C.sub.1-10 hydrocarbon aliphatic radical, (b) a C.sub.6-10 hydrocarbon aliphatic radical substituted by C.sub.6-10 aryl or by C.sub.6-10 aryl substituted by 1-3 halogen atoms, a phenyl group, 1-3 C.sub.1-4 alkyl groups or a chloromethyl, fluoromethyl, trifluoromethyl, carboxy, hydroxy or C.sub.1-4 alkoxy group; (c) C.sub.4-10 cycloalkyl, (d) C.sub.4-10 cycloalkyl substituted by C.sub.1-4 alkyl, (e) C.sub.6-10 aryl, (f) C.sub.6-10 aryl substituted by 1-3 halogen atoms, a phenyl group, 1-3 C.sub.1-4 alkyl groups or a chloromethyl, fluoromethyl, trifluoromethyl, carboxy, hydroxy or C.sub.1-4 alkoxy group; or (h) an aromatic heterocycle of 5 or 6 ring atoms one of which is O, N or S; andR.sub.3 is OH or OR; and, when R.sub.1 is hydrogen, the salts thereof with physiologically compatible bases, are effective as antihypertensive, bronchiodilators, thrombocyte aggregation inhibitors, inter alia.

9. 发明授权

US4689426A 5-alkylidene-2-halo-4-substituted-2-cyclopentenone and process for production thereof 失效
标题翻译： 5-亚烷基-2-卤代-4-取代-2-环戊烯酮及其制备方法
公开(公告)号：US4689426A
公开(公告)日：1987-08-25
申请号：US628107
申请日：1984-07-05
申请人： Satoshi Sugiura , Toshio Tanaka , Seizi Kurozumi
发明人： Satoshi Sugiura , Toshio Tanaka , Seizi Kurozumi
IPC分类号： C07C405/00 , C07C177/00
CPC分类号： C07C405/00
摘要： Novel 5-alkylidene-2-halo-4-substituted-2-cyclopentenone and process for production thereof. The novel 5-alkylidene-2-halo-4-substituted-2-cyclopentenones are represented by the following formula (I): ##STR1## wherein R.sub.a represents a substituted or unsubstituted aliphatic hydrocarbon group having 1 to 12 carbon atoms or a substituted or unsubstituted phenyl group, R.sub.b represents a substituted or unsubstituted aliphatic hydrocarbon group having 1 to 12 carbon atoms, and X represents a halogen atom. The novel cyclopentenones possess excellent pharmaceutical activities including anti-tumor activity, antiviral activity and antimicrobial activity.
摘要翻译：新型5-亚烷基-2-卤代-4-取代-2-环戊烯酮及其制备方法。新型5-亚烷基-2-卤代-4-取代-2-环戊烯酮由下式（I）表示：其中R a表示取代或未取代的碳原子数为1至12的脂族烃基或取代或未取代的苯基，Rb表示取代或未取代的碳原子数1〜12的脂肪族烃基，X表示卤素原子。新型环戊烯酮具有优异的药物活性，包括抗肿瘤活性，抗病毒活性和抗菌活性。

10. 发明授权

US4668814A Interphenylene carbacyclin derivatives 失效
标题翻译：亚氨基碳环链衍生物
公开(公告)号：US4668814A
公开(公告)日：1987-05-26
申请号：US690803
申请日：1985-01-11
申请人： Paul A. Aristoff
发明人： Paul A. Aristoff
IPC分类号： C07C405/00 , C07C177/00
CPC分类号： C07C405/0083
摘要： A compound of the formula ##STR1## and intermediates useful in preparing same.
摘要翻译：式“化合物”及其制备中可用的中间体。

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