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1. 发明授权

US4540684A 3-Nitro-5-amide-1,4-dihydropyridines with positive inotropic activity 失效
标题翻译：具有正性肌力活性的3-硝基-5-酰胺-1,4-二氢吡啶
公开(公告)号：US4540684A
公开(公告)日：1985-09-10
申请号：US612093
申请日：1984-05-18
申请人： Jurgen Stoltefuss , Gerhard Franckowiak , Horst Boshagen , Siegfried Goldmann , Matthias Schramm , Gunter Thomas , Rainer Gross
发明人： Jurgen Stoltefuss , Gerhard Franckowiak , Horst Boshagen , Siegfried Goldmann , Matthias Schramm , Gunter Thomas , Rainer Gross
IPC分类号： A61K31/455 , A61P3/08 , A61P9/02 , A61P9/04 , C07D211/90 , C07D211/98 , A61K31/70 , C07D405/12
CPC分类号： C07D211/90
摘要： A 1,4-dihydropyridine derivative of the formula ##STR1## in which R and R.sub.1 each independently is hydrogen, C.sub.1 -C.sub.4 -alkyl, C.sub.1 to C.sub.12 -alkoxy, C.sub.1 -C.sub.4 -halogenoalkoxy, halogen, nitro, trifluoromethyl, ##STR2## X is oxygen or sulphur, R.sub.4 and R.sub.5 each independently is hydrogen, C.sub.1 -C.sub.4 -alkyl, C.sub.1 -C.sub.6 -alkoxy, halogen, trifluoromethyl, amino or nitro, andR.sub.2 and R.sub.3 each independently is hydrogen, a C.sub.1 -C.sub.10 -alkyl, C.sub.2 -C.sub.10 -alkenyl or C.sub.3 -C.sub.10 -alkinyl radical which is optionally substituted by halogen, hydroxyl, C.sub.1 -C.sub.4 -alkoxy, amino, mono- and di-C.sub.1 -C.sub.4 -alkylamino, carbo-C.sub.1 -C.sub.6 -alkoxy and/or nitro, a C.sub.3 to C.sub.6 -membered cycloalkyl radical, a phenyl radical which is optionally substituted by C.sub.1 -C.sub.4 -alkyl, C.sub.1 -C.sub.6 -alkoxy, halogen, amino and/or nitro, or a phenyl-C.sub.1 -C.sub.3 -alkyl radical, or a carbohydrate radical which is optionally bonded via a C.sub.1 -C.sub.8 -alkyl chain to the amide nitrogen atomor a pharmaceutically acceptable acid addition salt thereof, which improves the contractility of the heart, raises the blood pressure, lowers the blood sugar, reduces the swelling of mucous membranes and affects the salt and fluid balances of a patient.
摘要翻译：其中R和R 1各自独立地为氢，C 1 -C 4 - 烷基，C 1 -C 12 - 烷氧基，C 1 -C 4卤代烷氧基，卤素，硝基，三氟甲基， X是氧或硫，R4和R5各自独立地是氢，C1-C4-烷基，C1-C6-烷氧基，卤素，三氟甲基，氨基或硝基，R2和R3各自独立地是氢，C1-C10 - 烷基，C 2 -C 10 - 烯基或C 3 -C 10 - 炔基，其任选被卤素，羟基，C 1 -C 4 - 烷氧基，氨基，单 - 和二-C 1 -C 4 - 烷基氨基，C 1 -C 6 - 和/或硝基，C3至C6元环烷基，任选被C 1 -C 4 - 烷基，C 1 -C 6 - 烷氧基，卤素，氨基和/或硝基取代的苯基，或苯基-C 1 -C 3 - 烷基或通过C1-C8烷基链任选与酰胺氮原子键合的碳水化合物基团或其药学上可接受的酸加成盐，其改善心脏的收缩力，使血压升高 ure，降低血糖，减少粘膜肿胀，影响患者的盐和液体平衡。

2. 发明授权

US4628107A Intermediate 8-carboxaldehyde-(-chromone and -thiochromone) derivatives 失效
标题翻译：中间体8-甲醛 - （ - 色酮和硫代色酮）衍生物
公开(公告)号：US4628107A
公开(公告)日：1986-12-09
申请号：US750571
申请日：1985-06-28
申请人： Siegfried Goldmann , Gerhard Franckowiak , Matthias Schramm , Gunter Thomas , Rainer Gross
发明人： Siegfried Goldmann , Gerhard Franckowiak , Matthias Schramm , Gunter Thomas , Rainer Gross
IPC分类号： C07D211/90 , C07D311/22 , C07D311/24 , C07D311/30 , C07D335/06 , C07D405/04 , C07D409/04 , C07D409/14 , C07D405/06 , C07D405/12 , C07D409/06 , C07D409/12
CPC分类号： C07D335/06 , C07D211/90 , C07D311/22 , C07D311/24 , C07D311/30 , C07D405/04 , C07D409/04 , C07D409/14
摘要： Novel chromone-8-aldehydes and thiochromone-8-aldehydes, useful in making pharmaceutically active dihydropyridines, of the formula ##STR1## in which R.sub.1 represents hydrogen, a C.sub.1 -C.sub.10 aliphatic hydrocarbon radical, a C.sub.1 -C.sub.10 alkyl carboxylate, or an aromatic or heteroaromatic ring which optionally has 1-5 identical or different halogen, C.sub.1 -C.sub.10 -alkyl, C.sub.1 -C.sub.10 -alkoxy, C.sub.1 -C.sub.10 -alkylthio, C.sub.1 -C.sub.10 -alkylsulphinyl, cyano, hydroxyl, nitro, C.sub.1 -C.sub.5 -monofluoroalkyl or polyfluoroalkyl, C.sub.1 -C.sub.5 monofluoroalkoxy or polyfluoroalkoxy, C.sub.1 -C.sub.6 monofluoroalkylthio or polyfluoroalkylthio, amino, C.sub.1 -C.sub.5 -monoalkylamino or C.sub.1 -C.sub.5 dialkylamino substituents,R.sub.2 represents hydrogen or 1 to 3 halogen atoms, A represents a single bond, a C.sub.1 -C.sub.20 alkylene chain or a C.sub.2 -C.sub.20 alkylene chain which can optionally be interrupted by oxygen or sulphur, andX represents oxygen or sulphur,are made from corresponding compounds which in 8-position carry an ester or olefinic radical.
摘要翻译：可用于制备药物活性二氢吡啶的新颖的色酮-8-醛和硫色酮-8-醛，其具有式“IMAGE”，其中R 1表示氢，C 1 -C 10脂族烃基，C 1 -C 10烷基羧酸酯或芳族或任选具有1-5个相同或不同的卤素，C 1 -C 10 - 烷基，C 1 -C 10 - 烷氧基，C 1 -C 10 - 烷硫基，C 1 -C 10 - 烷基亚磺酰基，氰基，羟基，硝基，C 1 -C 5 - 单氟烷基或多氟烷基，C 1 -C 5单氟烷氧基或多氟烷氧基，C 1 -C 6单氟烷硫基或多氟烷硫基，氨基，C 1 -C 5单烷基氨基或C 1 -C 5二烷基氨基取代基，R 2表示氢或1至3个卤素原子，A表示单键，亚烷基链或可任选被氧或硫中断的C 2 -C 20亚烷基链，X表示氧或硫，由相应的8-位带有酯或烯基的化合物制成。

3. 发明授权

US4772612A Circulation-active 1,4-dihydropyridines 失效
标题翻译：循环活性1,4-二氢吡啶类
公开(公告)号：US4772612A
公开(公告)日：1988-09-20
申请号：US870042
申请日：1986-06-03
申请人： Siegfried Goldmann , Jurgen Stoltefuss , Gerhard Franckowiak , Rainer Gross , Matthias Schramm , Gunter Thomas
发明人： Siegfried Goldmann , Jurgen Stoltefuss , Gerhard Franckowiak , Rainer Gross , Matthias Schramm , Gunter Thomas
IPC分类号： A61K31/4427 , A61K31/443 , A61K31/4433 , A61K31/455 , A61P9/00 , A61P9/04 , A61P9/08 , A61P9/12 , C07D211/90 , C07D333/00 , C07D401/12 , C07D405/12 , C07D409/12 , C07D491/04 , C07D491/048
CPC分类号： C07D409/12 , C07D211/90 , C07D491/04
摘要： Novel circulation active dihydropyridines of the formula ##STR1## in which X is CO, SO.sub.2 or CONH,R.sup.4 is H, OH, alkyl, halogen, acyloxy, alkoxyalkoxy, aralkyloxy, or together with R.sup.5 forms a heterocyclic ring, andthe other radicals are conventional in the dihydropyridine art,and pharmaceutically acceptable salts thereof.
摘要翻译：其中X为CO，SO 2或CONH，R 4为H，OH，烷基，卤素，酰氧基，烷氧基烷氧基，芳烷氧基或与R 5一起形成杂环的新型循环活性二氢吡啶类化合物，其中X为CO，SO2或CONH，在二氢吡啶领域中是常规的，及其药学上可接受的盐。

4. 发明授权

US4540789A Circulation-active novel chromone-and thiochromone-substituted 1,4-dihydropyridines 失效
标题翻译：循环活性新型色酮和硫色酮取代的1,4-二氢吡啶
公开(公告)号：US4540789A
公开(公告)日：1985-09-10
申请号：US589436
申请日：1984-03-14
申请人： Siegfried Goldmann , Gerhard Franckowiak , Matthias Schramm , Gunter Thomas , Rainer Gross
发明人： Siegfried Goldmann , Gerhard Franckowiak , Matthias Schramm , Gunter Thomas , Rainer Gross
IPC分类号： A61K31/435 , A61K31/443 , A61K31/4433 , A61K31/455 , A61P3/08 , A61P9/02 , A61P9/04 , A61P27/16 , C07D211/90 , C07D405/04 , C07D409/04 , C07D409/14 , C07D405/06
CPC分类号： C07D405/04 , C07D211/90 , C07D409/04 , C07D409/14
摘要： Dihydropyridines of the formula ##STR1## in which R.sup.1, R.sup.2, R.sup.5, R.sup.6, R.sup.7 and R.sup.8 can be hydrogen or various halogen or organic radicals,R.sup.4 is an optionally substituted hydrocarbon radical,A is a direct bond, an alkylene chain with 1 to 20 C atoms or an alkenylene chain with 2 to 20 atoms, the chains being optionally interrupted by O or S,X is O or S andY is a direct bond, O, S, -NH- or -N- alkyl with 1 to 8 C atoms,or a pharmaceutically acceptable salt thereof, are useful as cardiotonic agents for improving heart contractility, antihypotonic agents, for lowering the blood sugar level, for detumescing mucous membranes and for influencing the salt and liquid balance.
摘要翻译：其中R 1，R 2，R 5，R 6，R 7和R 8可以是氢或各种卤素或有机基团，R 4是任选取代的烃基，A是直接键，具有1至 20个C原子或具有2至20个原子的亚链烯基，链任选地被O或S间隔，X是O或S，Y是直接键，O，S，-NH-或-N-烷基，具有1至 8 C原子或其药学上可接受的盐可用作改善心脏收缩力的强心剂，抗低血糖剂，降低血糖水平，用于消肿粘膜和影响盐和液体平衡。

5. 发明授权

US4895855A Mixture of different dihydropyridines 失效
标题翻译：不同二氢吡啶的混合物
公开(公告)号：US4895855A
公开(公告)日：1990-01-23
申请号：US806160
申请日：1985-12-06
申请人： Siegfried Goldmann , Horst Boshagen , Friedrich Bossert , Gerhard Franckowiak , Horst Meyer , Jurgen Stoltefuss , Rainer Gross , Matthias Schramm , Gunter Thomas
发明人： Siegfried Goldmann , Horst Boshagen , Friedrich Bossert , Gerhard Franckowiak , Horst Meyer , Jurgen Stoltefuss , Rainer Gross , Matthias Schramm , Gunter Thomas
IPC分类号： C07D211/90 , A61K31/435 , A61K31/44 , A61K31/455 , A61P9/08 , A61P9/10 , A61P43/00 , C07D491/044 , C07D491/048 , C07D495/04
CPC分类号： A61K31/44
摘要： A composition effective for treating circulation disorders comprises a mixture of ##STR1## wherein the variables can have varied meetings. I are inotropic and II are vasodilating but, whereas the ingredients in the combination would be expected to be antagonistic, they are reinforcing.
摘要翻译：有效治疗循环障碍的组合物包含（I）和（II）的混合物，其中变量可以有不同的会议。我是变力和II是血管舒张，但是组合中的成分预计是对抗性的，它们是加强的。

6. 发明授权

US4532248A Method of combatting coronary and vascular diseases 失效
标题翻译：打击冠心病和血管疾病的方法
公开(公告)号：US4532248A
公开(公告)日：1985-07-30
申请号：US398034
申请日：1982-07-14
申请人： Gerhard Franckowiak , Horst Boshagen , Friedrich Bossert , Siegfried Goldmann , Horst Meyer , Egbert Wehinger , Jurgen Stoltefuss , Matthias Schramm , Gunter Thomas , Robertson Towart
发明人： Gerhard Franckowiak , Horst Boshagen , Friedrich Bossert , Siegfried Goldmann , Horst Meyer , Egbert Wehinger , Jurgen Stoltefuss , Matthias Schramm , Gunter Thomas , Robertson Towart
IPC分类号： A61K31/435 , A61K31/4427 , A61K31/4433 , A61K31/445 , A61K31/451 , A61K31/455 , A61K31/47 , A61K31/495 , A61K31/535 , A61P3/00 , A61P3/08 , A61P7/10 , A61P9/02 , A61P9/04 , A61P29/00 , C07D211/00 , C07D211/82 , C07D211/84 , C07D211/90 , C07D213/00 , C07D221/00 , C07D307/00 , C07D311/00 , C07D333/00 , C07D401/04 , C07D401/12 , C07D401/14 , C07D409/04 , C07D471/04 , C07D491/04 , C07D491/044 , C07D491/048 , C07D491/052 , C07D491/10 , C07D491/107 , C07D498/04 , A61K31/44
CPC分类号： C07D401/04 , C07D211/84 , C07D211/90 , C07D409/04 , C07D471/04 , C07D491/04 , C07D491/10
摘要： 1,4-Dihydropyridines of the formula ##STR1## in which n is 0,1 or 2, andR.sup.1 to R.sup.7 can have a wide variety of meanings, which possess inotropic action, and many of which are new, are useful in increasing the influx of Ca.sup.++ into cells, particularly in combatting coronary and vascular diseases, hypertension swelling in the mucous membranes and diseases involving increased blood sugar or an incorrect salt and fluid balance.
摘要翻译：其中n为0,1或2，且R1至R7可以具有多种含义，其具有各向异性作用，并且其中许多是新的，可用于增加其中n为0,1或2的1,4-二氢吡啶 Ca ++进入细胞，特别是与冠状动脉和血管疾病的对抗，粘膜中的高血压肿胀和血糖升高或不正确的盐和液体平衡的疾病。

7. 发明授权

US4555512A Circulation-active novel chromone- and thiochromone-substituted 1,4-dihydropyridine-lactones 失效
标题翻译：循环活性新型色酮和硫色酮取代的1,4-二氢吡啶内酯
公开(公告)号：US4555512A
公开(公告)日：1985-11-26
申请号：US589614
申请日：1984-03-14
申请人： Siegfried Goldmann , Friedrich Bossert , Matthias Schramm , Gunter Thomas , Rainer Gross
发明人： Siegfried Goldmann , Friedrich Bossert , Matthias Schramm , Gunter Thomas , Rainer Gross
IPC分类号： A61K31/435 , A61K31/44 , A61P3/00 , A61P3/08 , A61P9/02 , A61P9/04 , C07D307/66 , C07D491/04 , C07D491/048 , C07F7/08
CPC分类号： C07D491/04 , C07D307/66 , C07F7/0812
摘要： Dihydropyridines of the formula ##STR1## in which R.sup.1, R.sup.2, R.sup.5 and R.sup.6 can be hydrogen or various halogen or organic radicals,R.sup.4 is an optionally substituted hydrocarbon radical,A is a direct bond, a C.sub.1 -C.sub.20 -alkylene chain or a C.sub.2 -C.sub.20 -alkenylene chain, which chains are optionally interrupted by O or SX is O or S, andY is a direct bond, O, S, --NH--or--N-alkyl with 1 to 8 C atomsor a pharmaceutically acceptable salt,are useful as cardiotonic agents for improving heart contractility, antihypotonic agents, for lowering the blood sugar level, for detumescing mucous membranes and for influencing the salt and/or liquid balance.
摘要翻译：其中R 1，R 2，R 5和R 6可以是氢或各种卤素或有机基团，R 4是任选取代的烃基，A是直接键，C 1 -C 20亚烷基链或C 2 -C 20亚烷基链 -C 20亚烯基链，其任选地被O或SX中断，是O或S，Y是直接键，具有1至8个C原子的O，S，-NH-或N-烷基或其药学上可接受的盐可用作改善心脏收缩力的强心剂，抗低血糖剂，降低血糖水平，用于消肿粘膜和影响盐和/或液体平衡。

8. 发明授权

US4762853A 1-oxo-1,3,4,7-tetrahydrobenzo[C]furans 失效
标题翻译： 1-氧代-1,3,4,7-四氢苯并[C]呋喃
公开(公告)号：US4762853A
公开(公告)日：1988-08-09
申请号：US917875
申请日：1986-10-10
申请人： Siegfried Goldmann , Matthias Schramm , Gunter Thomas , Rainer Gross
发明人： Siegfried Goldmann , Matthias Schramm , Gunter Thomas , Rainer Gross
IPC分类号： A61K31/365 , A61K31/38 , A61K31/381 , A61K31/382 , A61K31/44 , A61K31/443 , A61K31/4433 , A61P3/00 , A61P3/08 , A61P9/00 , A61P9/02 , A61P9/04 , C07D307/88 , C07D333/72 , C07D335/00 , C07D405/04 , C07D409/04 , C07D407/02 , A61K31/35
CPC分类号： C07D405/04 , C07D307/88 , C07D409/04
摘要： 1-Oxo-1,3,4,7-tetrahydrobenzofuranes of the formula ##STR1## in which X is O or S,R is optionally substituted phenyl or heteroaryl,R.sup.1 is OH, monoalkylamino or dialkylamino, andR.sup.2 is an acyl or esterified carboxy radical,or pharmacologically acceptable salts thereof, which are active in circulation, e.g. they increase myocardial contractility, increase the flow of Ca.sup.2+ into the cell, increase blood pressure, reduce blood sugar, reduce swelling of mucous membranes and affect the salt and/or fluid balance.
摘要翻译：其中X为O或S，R为任选取代的苯基或杂芳基，R 1为OH，单烷基氨基或二烷基氨基，R 2为酰基或酯化的式羧基或其药理学上可接受的盐，其在循环中是有活性的，例如它们增加心肌收缩力，增加Ca2 +流入细胞，增加血压，降低血糖，减少粘膜肿胀并影响盐和/或液体平衡。

9. 发明授权

US4642310A Circulation-active tetrahydrothienopyridines 失效
标题翻译：循环活性四氢噻吩并吡啶
公开(公告)号：US4642310A
公开(公告)日：1987-02-10
申请号：US716876
申请日：1985-03-28
申请人： Siegfried Goldmann , Matthias Schramm , Gunter Thomas , Rainer Gross
发明人： Siegfried Goldmann , Matthias Schramm , Gunter Thomas , Rainer Gross
IPC分类号： A61K31/435 , A61K31/44 , A61K31/535 , A61P9/00 , C07D211/90 , C07D409/04 , C07D493/04 , C07D495/04 , C07D495/06 , A61K31/38 , C07D417/02 , C07D513/04
CPC分类号： C07D409/04 , C07C327/00 , C07D211/90 , C07D495/04
摘要： Tetrahydrothienopyridines of the formula ##STR1## in which R is optionally substituted aryl or heterocyclyl,R.sup.1 is an organic radical, andR.sup.2, R.sup.3 and R.sup.4 each independently is hydrogen or an organic radical, or pharmaceutically acceptable salts thereof, which are coronary active, hypotensive, anti-diabetic and salt balance restoring.
摘要翻译：其中R是任选取代的芳基或杂环基，R 1是有机基团，并且R 2，R 3和R 4各自独立地是氢或有机基团或其药学上可接受的盐，它们是冠状动脉，低血压的四氢噻吩并吡啶，抗糖尿病和盐平衡恢复。

10. 发明授权

US4647568A Circulation-active hydroxy-tetra-hydropyridinelactones 失效
公开(公告)号：US4647568A
公开(公告)日：1987-03-03
申请号：US673296
申请日：1984-11-20
申请人： Klaus Gorlitzer , Ulrich Bartke , Siegfried Goldmann , Matthias Schramm , Gunter Thomas , Rainer Gross
发明人： Klaus Gorlitzer , Ulrich Bartke , Siegfried Goldmann , Matthias Schramm , Gunter Thomas , Rainer Gross
IPC分类号： A61K31/435 , A61K31/47 , A61K31/505 , A61P3/00 , A61P3/08 , A61P9/04 , C07D211/90 , C07D491/04 , C07D491/048 , C07F7/10 , A61K31/455 , A61K31/535 , A61K31/695
CPC分类号： C07D491/04 , C07D211/90
摘要： Hydroxytetrahydropyridinelactones of the formula ##STR1## in which R represents a phenyl, naphthyl, thienyl, furyl, pyrryl, pyrazolyl, imidazolyl, oxazolyl, isoxazolyl, thiazolyl, pyridyl, pyridazinyl, pyrimidyl, pyrazinyl, quinolyl, isoquinolyl, indolyl, benzimidazolyl, quinazolyl, quinoxalyl, thionaphthenyl, isothionaphthenyl, chromonyl, thiochromonyl, chromenyl, thiochromenyl, benzoxadiazolyl or benzthiadiazolyl radical, and the stated radicals may carry 1 to 3 identical or different substituents from the group comprising C.sub.1 -C.sub.20 -alkyl, C.sub.2 -C.sub.20 -alkenyl, C.sub.2 -C.sub.20 -alkinyl, C.sub.1 -C.sub.20 -alkoxy, fluorine, chlorine, bromine, iodine, trifluoromethyl, monofluoro-C.sub.1 -C.sub.10 -alkoxy, polyfluoro-C.sub.1 -C.sub.10 -alkoxy, hydroxyl, amino, mono-C.sub.1 -C.sub.10 -alkylamino, di-C.sub.1 -C.sub.10 -alkylamino, nitro, cyano, azido, carboxyl, carb-C.sub.1 -C.sub.10 -alkoxy, carboxamido, sulphonamido, SO.sub.m -alkyl (m=0 to 2, 1 to 20 C atoms), phenyl, benzyl, benzyloxy or benzylthio, it being possible for the 4 last-mentioned substituents to carry 1 to 3 radicals from the group comprising C.sub.1 -C.sub.5 -alkyl, C.sub.1 -C.sub.5 -alkoxy, C.sub.1 -C.sub.5 -alkylthio, fluorine, chlorine, bromine, iodine, cyano, nitro, azido, hydroxyl, trifluoromethyl, amino, C.sub.1 -C.sub.6 -alkylamino or di-C.sub.1 -C.sub.6 -alkylamino,R.sup.1 represents a straight-chain, branched or cyclic saturated or unsaturated hydrocarbon radical which has 1-20 C atoms, may be interrupted in the chain by 1 or 2 oxygen or sulphur atoms and may be optionally substituted by one or more fluorine atoms, NO.sub.2, C.sub.3 -C.sub.12 -trialkyl-silyl, hydroxyl, chlorine, bromine, iodine or cyano,R.sup.2 represents hydrogen, --NH.sub.2, --CHO, cyano, --CH.sub.2 OH or a straight-chain or branched saturated or unsaturated hydrocarbon radical having 1 to 8 C atoms,R.sup.3 represents hydrogen or a straight-chain or branched C.sub.1 -C.sub.10 -alkyl radical which may be interrupted in the alkyl chain by one or two oxygen atoms and may be optionally substituted by fluorine, chlorine, bromine, iodine, --CN, --NH.sub.2, --OH or morpholino, which can be used as cardiotonics for improving the contractility of the heart. Moveover, they increase the flow of Ca.sup.++ into the cells and can therefore be employed as antihypotonics, for lowering the blood sugar level, for reducing the swelling of mucous membranes and for influencing the salt balance and/or fluid balance.

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