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1. 发明专利

HRP960009A2 9-SUBSTITUTED 2-(2-N-ALKOXYPHENYL)-PURIN-6-ONES 未知
公开(公告)号：HRP960009A2
公开(公告)日：1997-12-31
申请号：HRP960009
申请日：1996-01-08
申请人： MATTHIAS SCHRAMM
发明人： SCHRAMM MATTHIAS
IPC分类号： C07D473/34 , A61K31/52 , A61K31/522 , A61K31/535 , A61K31/63 , A61K31/655 , A61P7/02 , A61P9/00 , A61P13/02 , A61P15/00 , A61P29/00 , A61P43/00 , C07D295/26 , C07D473/00 , C07D473/30
摘要： 9-Substd. 2-(2-alkoxyphenyl)-purin-6-ones of formula (I) and their tautomers and salts are new: A = -CR1R5-CR2R3-R4, -CR6R7R8 or -(CH2)aMe; a = 9-15; R1 = 2-10C alkyl or phenyl (2-10C) alkyl opt. ring-substd. by halogen, NO2, CN, 1-6C alkyl or SO2NR9R10; R9 and R10 = H, phenyl, 1-6C alkyl or 1-6C hydroxyalkyl, or NR9R10 is a 5- or 6-membered satd. ring which contains 0-2 further heteroatoms (S, N and/or O) and is opt. substd. via a free N atom by 1-6C alkyl or hydroxyalkyl; one of the above alkyl gps. (ambiguous) is opt. substd. by NR11R12; R11 and R12 = as defined for R9 and R10; R2 = H, azido, 1-6C alkyl, OR13, OSO2R14 or NR15R16; R3 = H; or R2+R3 = O or NOR20; R13 = H, a protecting gp., 1-6C acyl, benzoyl, or 1-6C alkyl opt. substd. by COOH, 2-6C alkoxycarbonyl or CONR17R18; R17 and R18 = H or 1-4C alkyl; R14 = 1-4C alkyl or phenyl; R15 and R16 = H, protecting gps., 1-6C alkyl, 1-6C acyl, CHO, benzoyl or SO2R19; R19 = 1-4C alkyl or phenyl; R20 = H or 1-6C alkyl opt. substd. by phenyl or NR21R22; R21 and R22 = H, phenyl or 1-6C alkyl; R4 = H or 1-4C alkyl; R5 and R8 = H or 1-3C alkyl; R6 = H or 1-5C alkyl or hydroxyalkyl; R7 = 2-8C alkyl substd. by NR23R24; R23 and R24 = H, 1-5C alkyl (opt. substd. by OH) or phenyl (1-5C) alkyl ring-substd. by SO2NR25R26; R25 and R26 = gps. as defined for R9 and R10; D = H or SO2NR27R28; R27 and R28 = gps. as defined for R9 and R10; E = 1-8C alkyl.

2. 发明授权

US5721238A 2,8-disubstituted quinazolinones 失效
标题翻译： 2,8-二取代喹唑啉酮
公开(公告)号：US5721238A
公开(公告)日：1998-02-24
申请号：US584865
申请日：1996-01-11
申请人： Fred Robert Heiker , Ulrich Niewohner , Wolfgang Hartwig , Helmuth Schutz , Erwin Bischoff , Elisabeth Perzborn , Matthias Schramm
发明人： Fred Robert Heiker , Ulrich Niewohner , Wolfgang Hartwig , Helmuth Schutz , Erwin Bischoff , Elisabeth Perzborn , Matthias Schramm
IPC分类号： A61K31/505 , A61K31/517 , A61K31/535 , A61K31/655 , A61P7/02 , A61P9/06 , A61P9/08 , A61P9/10 , A61P13/08 , A61P29/00 , A61P43/00 , C07D239/91 , C07D405/04 , C07D413/12 , C07D413/14 , C07D239/80
CPC分类号： C07D405/04 , C07D239/91
摘要： 2,8-Disubstituted quinazolinones are prepared by first subjecting the quinazolinone basic skeleton to condensation by customary reactions and then introducing the desired substituents into the 8-position. The compounds are suitable as active compounds in medicaments, in particular for the treatment of inflammations, thromboembolic diseases and cardiovascular diseases.
摘要翻译：通过首先使喹唑啉酮碱性骨架通过常规反应冷凝，然后将所需的取代基引入8-位来制备2,8-二取代喹唑啉酮。该化合物适合作为药物中的活性化合物，特别是用于治疗炎症，血栓栓塞性疾病和心血管疾病。

3. 发明授权

US4886820A Dihydropyridine combination product comprising a dihydropyridine compound and a cardioactive nitrate 失效
标题翻译：包含二氢吡啶化合物和心脏活性硝酸盐的二氢吡啶组合产物
公开(公告)号：US4886820A
公开(公告)日：1989-12-12
申请号：US274182
申请日：1988-11-03
申请人： Rainer Gross , Matthias Schramm
发明人： Rainer Gross , Matthias Schramm
IPC分类号： A61K31/34 , A61K31/04 , A61K31/44 , A61K31/455 , A61P9/08 , A61P9/10
CPC分类号： A61K31/44
摘要： A solid medicament formulation which can be administered orally, comprising 1 to 40 mg of a dihydropyridine of the formula ##STR1## in which R.sup.1 and R.sup.3 are always different from one another and represent alkyl which has 1 to 12 carbon atoms and which is optionally substituted once or several times by fluorine or chlorine or which is optionally interrupted by an oxygen atom in the chain, andA represents the radical ##STR2## R.sup.2 representing one or two substituents from the group consisting of nitro, chlorine and trifluoromethyl, or represents and 0.1 to 100 mg of a cardioactive nitrate. The composition is cardio-active and the patient's tendency toward nitrate tolerance is reduced.
摘要翻译：可以口服给药的固体药物制剂，其包含1至40mg式“IMAGE”的二氢吡啶，其中R 1和R 3总是彼此不同，并且表示具有1至12个碳原子并且任选被取代的烷基一次或几次用氟或氯或任选地被链中的氧原子中断，并且A代表表示一个或两个来自硝基，氯和三氟甲基的取代基的基团，或表示和0.1至100mg的心脏活性硝酸盐。该组合物是有活力的，并且患者对耐硝酸盐耐受性的倾向降低。

4. 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。

5. 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。

6. 发明授权

US5008279A Circulation-active fluoromethoxyphenyl dihydropyridine compounds 失效
标题翻译：循环活性氟甲氧基苯基二氢吡啶化合物
公开(公告)号：US5008279A
公开(公告)日：1991-04-16
申请号：US263671
申请日：1988-10-27
申请人： Gerhard Franckowiak , Jurgen Stoltefuss , Martin Bechem , Rainer Gross , Michael Kayser , Siegbert Hebisch , Matthias Schramm
发明人： Gerhard Franckowiak , Jurgen Stoltefuss , Martin Bechem , Rainer Gross , Michael Kayser , Siegbert Hebisch , Matthias Schramm
IPC分类号： A61K31/445 , A61K31/451 , A61P9/08 , C07D211/90 , C07D401/12
CPC分类号： C07D401/12 , C07D211/90
摘要： Circulation-active fluoromethoxyphenyldihydropyridines of the formula ##STR1## in which X stands for hydrogen or fluorine andR stands for straight-chain, branched or cyclic alkyl or alkenyl having 2 to 12 carbon atoms which can be interrupted by 1 to 2 oxygen and/or sulphur atoms in the chain, and which can be monosubstituted or polysubstituted(a) by hydroxyl, aryl having 6 to 12 carbon atoms, aryloxy having 6 to 12 carbon atoms, where the aryl radical is again substituted by alkyl having up to 4 carbon atoms, alkoxy having up to 4 carbon atoms or halogen, the substituents being identical or different, or(b) by carboxyl, alkoxycarbonyl having up to 6 carbon atoms, pyridyl, piperidyl, pyrimidyl, acyloxy having up to 7 carbon atoms, sulphamoyl, carbamoyl, halogen or cyano, the substituents being identical or different, or(c) by an amino group, where the amino group can carry one or two identical or different substituents from the group consisting of alkyl having up to 6 carbon atoms, benzyl, phenyl or acyl having up to 7 carbon atoms,and salts thereof.
摘要翻译：式（I）的循环活性氟甲氧基苯基二氢吡啶，其中X代表氢或氟，R代表可被1至2个氧中断的具有2至12个碳原子的直链，支链或环状烷基或链烯基和/或链中的硫原子，并且其可以被羟基，具有6至12个碳原子的芳基，具有6至12个碳原子的芳氧基单取代或多取代（a），其中芳基再次被具有至多 4个碳原子，具有至多4个碳原子的烷氧基或卤素，取代基相同或不同，或（b）由羧基，具有至多6个碳原子的烷氧基羰基，吡啶基，哌啶基，嘧啶基，具有至多7个碳原子的酰氧基，氨基甲酰基，氨基甲酰基，卤素或氰基，取代基相同或不同，或（c）氨基，其中氨基可以带有一个或两个相同或不同的取代基，由至多6个碳原子的烷基 ms，苄基，苯基或具有至多7个碳原子的酰基及其盐。

7. 发明授权

US4904665A Benzylaminoaryl-dihydropyridinelactones and their use in medicaments 失效
标题翻译：苄基氨基芳基 - 二氢吡啶内酯及其在药物中的用途
公开(公告)号：US4904665A
公开(公告)日：1990-02-27
申请号：US158184
申请日：1988-02-18
申请人： Siegfried Goldmann , Rainer Gross , Martin Bechem , Michael Kayser , Matthias Schramm , Siegbert Hebisch
发明人： Siegfried Goldmann , Rainer Gross , Martin Bechem , Michael Kayser , Matthias Schramm , Siegbert Hebisch
IPC分类号： A61K31/44 , A61P3/08 , A61P9/00 , A61P9/06 , A61P9/08 , A61P9/10 , C07D211/90 , C07D491/04 , C07D491/048
CPC分类号： C07D491/04 , C07D211/90
摘要： A benzylaminoaryl-dihydropyridinelactone compound of the formula (I) ##STR1## in which R.sup.1 represents hydrogen, halogen, cyano, nitro, C.sub.6 -C.sub.12 -aryl, C.sub.1 -C.sub.8 -alkyl, C.sub.1 -C.sub.8 -alkoxy, C.sub.1 -C.sub.6 -alkylthio, trifluoromethyl, trifluoromethoxy, trifluoromethylthio, difluoromethoxy, di-C.sub.1 -C.sub.5 -alkylamino, C.sub.1 -C.sub.6 -alkoxycarboxyl or C.sub.1 -C.sub.6 -alkylsulphonyl,R.sup.2 represents hydrogen, or represents a straight-chain, branched or cyclic, saturated or unsaturated hydrocarbon radical having up to 10 carbon atoms which is optionally substituted by C.sub.1 -C.sub.6 -alkoxy, C.sub.1 -C.sub.6 -alkylthio, C.sub.1 -C.sub.6 -alkylsulphonyl, halogen, cyano, hydroxyl, pyridyl, thienyl, pyrimidyl, piperidinyl, phenyl or an amino group, where the amino group carries two identical or different substituents from the series comprising C.sub.1 -C.sub.5 -alkyl, phenyl or benzyl,R.sup.3 represents C.sub.1 -C.sub.5 -alkyl, or represents cyano, hydroxymethyl or formyl, andR.sup.4 represents hydrogen, halogen, C.sub.1 -C.sub.5 -alkyl or trifluoromethyl,and its isomers, isomeric mixtures, racemates or optical antipodes, and physiologically acceptable salts thereof. The compound being useful to improve the contractility of the heart and the tonus of the smooth muscles.
摘要翻译：式（I）的苄基氨基芳基 - 二氢吡啶内酯化合物其中R 1表示氢，卤素，氰基，硝基，C 6 -C 12 - 芳基，C 1 -C 8 - 烷基，C 1 -C 8 - 烷氧基，C 1 -C 6 - 烷硫基，三氟甲基，三氟甲氧基，三氟甲硫基，二氟甲氧基，二-C 1 -C 5烷基氨基，C 1 -C 6 - 烷氧基羧基或C 1 -C 6烷基磺酰基，R 2表示氢，或表示直链，支链或环状饱和或不饱和烃具有至多10个碳原子的基团，其任选被C 1 -C 6 - 烷氧基，C 1 -C 6 - 烷硫基，C 1 -C 6 - 烷基磺酰基，卤素，氰基，羟基，吡啶基，噻吩基，嘧啶基，哌啶基，苯基或氨基取代，其中氨基从包含C 1 -C 5 - 烷基，苯基或苄基的系列中携带两个相同或不同的取代基，R 3表示C 1 -C 5 - 烷基，或表示氰基，羟甲基或甲酰基，R 4表示氢，卤素，C 1 -C 5 - 烷基或三氟甲基，及其异构体，异构体混合物，外消旋体或光学抗体 es及其生理上可接受的盐。该化合物可用于改善心脏和平滑肌紧张的收缩性。

8. 发明授权

US4898865A [4-(6-Oxo-1,4,5,6-tetrahydro-3-pyridazinyl) anilino hexyl 1,4-dihydro-2,6 Di methyl 5 nitro 4 aryl pyridine 3-carboxylates 失效
标题翻译： [4-（6-氧代-1,4,5,6-四氢-3-哒嗪基）苯胺基己基1,4-二氢-2,6-二甲基-5-硝基4芳基吡啶3-羧酸酯
公开(公告)号：US4898865A
公开(公告)日：1990-02-06
申请号：US218759
申请日：1988-07-13
申请人： Gerhard Franckowiak , Martin Bechem , Michael Kayser , Rainer Gross , Matthias Schramm , Friedel Seuter , Elisabeth Perzborn , Gunther Thomas
发明人： Gerhard Franckowiak , Martin Bechem , Michael Kayser , Rainer Gross , Matthias Schramm , Friedel Seuter , Elisabeth Perzborn , Gunther Thomas
IPC分类号： A61K31/50 , A61P3/00 , A61P3/08 , A61P9/00 , C07D237/04 , C07D401/12 , C07D409/14 , C07D413/14 , C07D417/14
CPC分类号： C07D401/12 , C07D237/04
摘要： Circulation active nitrodihydropyridines of the formula ##STR1## in which R represents aryl which has 6 to 12 carbon atoms and can be substituted up to 4 times, identically or differently, by halogen, nitro, cyano, alkyl, alkoxy, alkylthio, in each case having up to 6 carbon atoms, trifluoromethyl, trifluoromethoxy, difluoromethoxy, trifluoromethylthio, difluoromethylenedioxy, trifluoroethylenedioxy or tetrafluoroethylenedioxy or by benzyl, benzyloxy or benzylthio, each of which is optionally substituted by halogen, nitro, cyano, trifuoromethyl, alkyl having up to 4 carbon atoms or alkoxy having up to 4 carbon atoms, or represents a heterocycle which is optionally substituted by halogen, phenyl or alkyl having up to 4 carbon atoms and is from the group consisting of pyrryl, thienyl, furyl, pyrazolyl, imidazolyl, oxazolyl, thiazolyl, pyridyl, pyrimidyl, pyridazinyl, quinolyl, benzoxadiazolyl, chromenyl or thiochromenyl, andn represents a number from 1 to 12,and physiologically acceptable salts thereof.
摘要翻译：具有式“IMAGE”的循环活性硝基二氢吡啶，其中R表示具有6至12个碳原子并且可以相同或不同地被卤素，硝基，氰基，烷基，烷氧基，烷硫基取代至多4次的芳基，具有至多6个碳原子，三氟甲基，三氟甲氧基，二氟甲氧基，三氟甲硫基，二氟亚甲二氧基，三氟亚乙二氧基或四氟亚乙二氧基或苄基，苄氧基或苄硫基，其各自任选被卤素，硝基，氰基，三氟甲基，具有至多4个碳原子的烷基或具有至多4个碳原子的烷氧基，或表示任选被卤素，苯基或具有至多4个碳原子的烷基取代的杂环，并且是由吡咯基，噻吩基，呋喃基，吡唑基，咪唑基，恶唑基，噻唑基，吡啶基，嘧啶基，哒嗪基，喹啉基，苯并二唑基，苯并二唑基，色烯基或硫代色烯基，n表示1〜12的数，生理学上可接受的其盐。

9. 发明授权

US4886816A Circulation-active dioxyalkylenearyl-dihydropyridines 失效
标题翻译：循环活性二氧杂环己烯基 - 二氢吡啶
公开(公告)号：US4886816A
公开(公告)日：1989-12-12
申请号：US190748
申请日：1988-05-05
申请人： Gerhard Franckowiak , Albrecht Marhold , Martin Bechem , Rainer Gross , Michael Kayser , Matthias Schramm , Gunther Thomas
发明人： Gerhard Franckowiak , Albrecht Marhold , Martin Bechem , Rainer Gross , Michael Kayser , Matthias Schramm , Gunther Thomas
IPC分类号： C07D317/46 , A61K31/335 , A61K31/357 , A61K31/36 , A61K31/44 , A61K31/443 , A61K31/4433 , A61K31/455 , A61K31/50 , A61P3/08 , A61P9/00 , A61P9/04 , A61P9/08 , A61P9/10 , C07D319/20 , C07D405/04 , C07D405/14 , C07D409/14 , C07D413/14 , C07D417/14 , C07D491/04 , C07D491/044 , C07D491/048
CPC分类号： C07D405/04 , C07D405/14 , C07D491/04
摘要： Circulation-active dihydropyridines of the formula ##STR1## in which R.sup.1 is H, CN, NO.sub.2 or --COOR.sup.7,R.sup.7 is H, alkyl or various other radicals,R.sup.2 and R.sup.4 each independently is alkyl or other radicals,R.sup.3 is H or optionally substituted alkyl,R.sup.5 completes a keto or ester group, andR.sup.6 is a direct bond or --CF.sub.2 -- or --CHF--,and physiologically acceptable salts thereof.
摘要翻译：其中R 1是H，CN，NO 2或-COOR 7，R 7是H，烷基或各种其它基团，R 2和R 4各自独立地是烷基或其它基团，R 3是H或任选被取代的具有通式“IMAGE”的循环活性二氢吡啶烷基，R5完成酮基或酯基团，并且R 6是直接键或-CF2-或-CHF-，及其生理上可接受的盐。

10. 发明授权

US4772611A Circulation-active 3-amino-dihydropyridines 失效
标题翻译：循环活性3-氨基 - 二氢吡啶
公开(公告)号：US4772611A
公开(公告)日：1988-09-20
申请号：US43656
申请日：1987-04-28
申请人： Jurgen Stoltefuss , Fred R. Heiker , Martin Bechem , Rainer Gross , Michael Kayser , Matthias Schramm , Gunter Thomas
发明人： Jurgen Stoltefuss , Fred R. Heiker , Martin Bechem , Rainer Gross , Michael Kayser , Matthias Schramm , Gunter Thomas
IPC分类号： A61K31/44 , A61K31/4427 , A61K31/4433 , A61K31/505 , A61P9/00 , C07D211/84 , C07D211/90 , C07D401/04 , C07D409/04 , C07D413/04 , C07D491/04 , C07D491/048 , A61K31/455
CPC分类号： C07D491/04 , C07D211/84 , C07D211/90
摘要： Novel cardioactive compounds of the formula ##STR1## in which R.sup.1 is alkyl, aryl or heterocyclic, preferably substituted phenyl,R.sup.2 is alkyl, preferably methyl,R.sup.3 is hydrogen, halogen, acyloxy or alkyl, preferably hydrogen, andR.sup.4 is phenyl, carbalkoxy or together with R.sup.3 forms a ring, preferably carbalkoxy,are produced by reducing the corresponding nitro compounds.
摘要翻译：式（IMAGE）的新型心脏活性化合物，其中R 1是烷基，芳基或杂环，优选取代的苯基，R 2是烷基，优选甲基，R 3是氢，卤素，酰氧基或烷基，优选氢，R 4是苯基，通过还原相应的硝基化合物与R3一起形成环，优选为烷氧基。

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