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公开(公告)号:US4258062A
公开(公告)日:1981-03-24
申请号:US43925
申请日:1979-05-30
IPC分类号: A61K31/13 , A61K20060101 , A61K31/135 , A61K31/165 , A61K31/36 , A61P3/06 , A61P7/02 , A61P9/00 , A61P9/06 , A61P9/12 , A61P25/00 , A61P25/02 , C07C20060101 , C07C67/00 , C07C213/00 , C07C217/32 , C07D317/06 , C07D317/54 , C07D317/58 , C07C93/06
CPC分类号: C07D317/58 , C07D303/24 , Y10S514/821
摘要: New phenoxy-amino-propanols of formula ##STR1## wherein R.sup.1 is alkenyl, alkynyl, alkoxyalkyl or alkenyloxyalkyl with 2-6 C atoms in each case or cycloalkyl with 3-8 C atoms; and R.sup.2 is alkyl or hydroxyalkyl with 1-6 C atoms in each case, cycloalkyl with 3-8 C atoms, aralkyl or aralkyl wherein the aryl radical is mono- to tri-substituted by alkyl, alkoxy, OH, F and/or Cl or mono-substituted by methylenedioxy, with a total of 7-15 C atoms in each case, and the physiologically acceptable acid addition salts thereof, exhibit various pharmacological properties including isoprenaline-antagonism on the heart rate and blood pressure.
摘要翻译: 其中R 1是具有2-6个C原子的链烯基,炔基,烷氧基烷基或烯氧基烷基,或者具有3-8个C原子的环烷基的新的苯氧基 - 氨基 - 丙醇; 并且R 2是每种情况下具有1-6个C原子的烷基或羟基烷基,具有3-8个C原子的环烷基,芳烷基或芳烷基,其中所述芳基被烷基,烷氧基,OH,F和/或Cl单取代至三取代 或者由亚甲二氧基单取代,在每种情况下总共具有7-15个C原子,并且其生理上可接受的酸加成盐具有包括对心率和血压的异丙肾上腺素拮抗作用的各种药理学性质。
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公开(公告)号:US4171370A
公开(公告)日:1979-10-16
申请号:US839487
申请日:1977-10-04
IPC分类号: A61K31/13 , A61K20060101 , A61K31/135 , A61K31/165 , A61K31/36 , A61P3/06 , A61P7/02 , A61P9/00 , A61P9/06 , A61P9/12 , A61P25/00 , A61P25/02 , C07C20060101 , C07C67/00 , C07C213/00 , C07C217/32 , C07D317/06 , C07D317/54 , C07D317/58
CPC分类号: C07D317/58 , C07D303/24 , Y10S514/821
摘要: New phenoxy-amino-propanols of formula ##STR1## wherein R.sup.1 is alkenyl, alkynyl, alkoxyalkyl or alkenyloxyalkyl with 2-6 C atoms in each case or cycloalkyl with 3-8 C atoms; and R.sup.2 is alkyl or hydroxyalkyl with 1-6 C atoms in each case, cycloalkyl with 3-8 C atoms, aralkyl or aralkyl wherein the aryl radical is mono- to tri-substituted by alkyl, alkoxy, OH, F and/or Cl or mono-substituted by methylenedioxy, with a total of 7-15 C atoms in each case, and the physiologically acceptable acid addition salts thereof, exhibit various pharmacological properties including isoprenaline-antagonism on the heart rate and blood pressure.
摘要翻译: 其中R 1是具有2-6个C原子的链烯基,炔基,烷氧基烷基或烯氧基烷基,或者具有3-8个C原子的环烷基的新的苯氧基 - 氨基 - 丙醇; 并且R 2是每种情况下具有1-6个C原子的烷基或羟基烷基,具有3-8个C原子的环烷基,芳烷基或芳烷基,其中所述芳基被烷基,烷氧基,OH,F和/或Cl单取代至三取代 或者由亚甲二氧基单取代,在每种情况下总共具有7-15个C原子,并且其生理上可接受的酸加成盐具有包括对心率和血压的异丙肾上腺素拮抗作用的各种药理学性质。
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公开(公告)号:US3989833A
公开(公告)日:1976-11-02
申请号:US520888
申请日:1974-11-04
IPC分类号: C07D473/34 , A61K20060101 , A61K31/52 , C07D20060101 , C07D235/00 , C07D239/00
摘要: Adenine derivatives of the formula ##SPC1##Wherein R is phenyl or thienyl, and the physiologically acceptable acid addition salts thereof, possess, with good compatibility, cardio-active properties and are produced by the reaction of a purine derivative of the formula ##SPC2##Wherein X is F, Cl, Br, I, SR.sub.1, SOR.sub.1, SO.sub.2 R.sub.1 or OSi(CH.sub.3).sub.3, R.sub.1 being alkyl of 1-4 carbon atoms, phenyl or benzyl, with an amine of the formula ##SPC3##Wherein R has the values given above, or a salt thereof.
摘要翻译: 式WHEREIN R是苯基或噻吩基的腺嘌呤衍生物及其生理学上可接受的酸加成盐具有良好的相容性,具有心脏活性的特性,并且通过式WHEREIN X的嘌呤衍生物与F,Cl ,Br,I,SR1,SOR1,SO2R1或OSi(CH3)3,R1为1-4个碳原子的烷基,苯基或苄基,与式WHEREIN R具有上述给出的值或其盐。
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公开(公告)号:US5104881A
公开(公告)日:1992-04-14
申请号:US595010
申请日:1984-03-29
IPC分类号: C07C65/24 , C07C65/28 , C07D471/04
CPC分类号: C07D471/04 , C07C65/24 , C07C65/28
摘要: New 2-arylimidazopyridines of the general formula I ##STR1## wherein --A.dbd.B-- is (a) --CH.dbd.N-- or (b) N.dbd.CH--,Ar is a phenyl radical, which, in case (a), is substituted by one or two alkynyloxy, cyanomethoxy, carboxymethoxy, and/or alkyloxycarbonylmethoxy groups, and can be substituted by one or two additional hydroxyl, alkyloxy, alkenyloxy and/or alkynyloxy groups, or which in case (b), is substituted by one to three hydroxyl, mercapto, and/or --Z--R groups, Z is --O--, --S-- or --SO-- andR is alkyl, alkenyl, alkynyl, hydroxyalkyl, cyanomethyl, carboxymethyl or alkyloxycarbonylmethyl, the alkyl, alkenyl, alkynyl and hydroxyalkyl groups each having up to 5 C atoms, but wherein in case (b), the phenyl radical is only substituted by hydroxyl or methoxy groups if it has at the same time at least one other substituent differing from these,and their physiologically acceptable salts show positive inotropic effects.
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公开(公告)号:US5276027A
公开(公告)日:1994-01-04
申请号:US964686
申请日:1992-10-22
申请人: Rochus Jonas , Michael Klockow , Joachim Leibrock , Hans-Jochen Schliep , Christoph Seyfried , Michael Wolf
发明人: Rochus Jonas , Michael Klockow , Joachim Leibrock , Hans-Jochen Schliep , Christoph Seyfried , Michael Wolf
IPC分类号: A61K31/54 , A61K31/549 , A61P9/04 , A61P9/08 , A61P11/00 , A61P11/06 , A61P25/24 , A61P25/26 , A61P25/28 , A61P29/00 , A61P43/00 , C07D285/16
CPC分类号: C07D285/16
摘要: Compounds of formula I ##STR1## in which R.sup.1 and R.sup.2 are each independently of one another H or A,R.sup.3 is H, OA or O--C.sub.m H.sub.2m+1-n X.sub.n,R.sup.4 is --O--C.sub.m H.sub.2m+1-n X.sub.n,X is F or Cl,A is alkyl having 1-6 C atoms,m is 1, 2, 3, 4, 5 or 6 andn is 1, 2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12 or 13, and their salts have positive ionitropic activity and vasodilating action, and promote circulation. In addition, the compounds can be employed for the treatment of asthmatic disease and memory disorders, and have anti-depressive and anti-inflammatory properties.
摘要翻译: 其中R1和R2各自独立地为H或A,R3为H,OA或O-CmH2m + 1-nXn,R4为-O-CmH2m + 1-nXn的式I化合物,其中X为 F或Cl,A是具有1-6个C原子的烷基,m是1,2,3,4,5或6,n是1,2,3,4,5,6,7,8,9,10, 11,12或13,其盐具有阳离子活性和血管扩张作用,促进循环。 此外,该化合物可用于治疗哮喘病和记忆障碍,并具有抗抑郁和抗炎特性。
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公开(公告)号:US4260628A
公开(公告)日:1981-04-07
申请号:US78855
申请日:1979-09-26
IPC分类号: A61K31/40 , A61K31/403 , A61K31/404 , A61P9/12 , C07D209/14
CPC分类号: C07D209/14
摘要: 2-Guanidinomethyl-indolines of the formula ##STR1## wherein R.sup.1 and R.sup.2 each independently is H or alkyl of 1-6 carbon atoms, and the physiologically acceptable acid addition salts thereof have good antihypertensive properties.This is a division of application Ser. No. 939,046 filed Sept. 1, 1978, now abandoned.
摘要翻译: 其中R1和R2各自独立地为H或1-6个碳原子的烷基,其生理学上可接受的酸加成盐具有良好的抗高血压性质。
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公开(公告)号:US5434149A
公开(公告)日:1995-07-18
申请号:US220657
申请日:1994-03-31
IPC分类号: A61K31/54 , A61P9/08 , A61P11/00 , A61P25/24 , A61P25/26 , A61P25/28 , A61P29/00 , A61P43/00 , C07D285/16 , C07D285/18 , C07D417/04 , C07D417/06
CPC分类号: C07D285/16 , C07D417/04
摘要: The present invention relates to thiadiazinones of the formula I ##STR1## having a phosphodiesterase-inhibiting action and which are suitable for combating cardiovascular and asthmatic disorders.
摘要翻译: 本发明涉及具有磷酸二酯酶抑制作用并且适于对抗心血管和哮喘病症的式I的噻二嗪酮。
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公开(公告)号:US4477454A
公开(公告)日:1984-10-16
申请号:US492909
申请日:1983-05-09
申请人: Rochus Jonas , Michael Kloft , Hanns Wurziger , Juergen Harting , Hans J. Enenkel , Klaus-Otto Minck , Hans-Jochen Schliep
发明人: Rochus Jonas , Michael Kloft , Hanns Wurziger , Juergen Harting , Hans J. Enenkel , Klaus-Otto Minck , Hans-Jochen Schliep
IPC分类号: A61K31/495 , A61K31/50 , A61P1/04 , A61P9/00 , A61P9/04 , A61P43/00 , C07C65/28 , C07D487/04 , C07D487/00
CPC分类号: C07D487/04 , C07C65/28
摘要: 2-Aryltetraazaindenes of the formula ##STR1## wherein --A-- is --N.dbd.CH--CH.dbd.N-- or --CH.dbd.N--N.dbd.CH--, Ar is unsubstituted phenyl or phenyl mono-, di- or tri-substituted by hydroxyl, mercapto, dialkylamino, trifluoromethyl and/or --Z--R groups, Z is --O--, --S-- or --SO-- and R is alkyl, alkenyl, alkynyl or cyanomethyl, the alkyl, alkenyl and alkynyl groups each having up to 5 C atoms, and their physiologically acceptable salts, exhibit blood pressure, myocardial contraction, and anti-ulcer activities.
摘要翻译: 其中-A-为-N = CH-CH = N-或-CH = NN = CH-,Ar为未取代的苯基或被羟基单,二或三取代的苯基, 巯基,二烷基氨基,三氟甲基和/或-ZR基团,Z是-O - , - S-或-SO-,R是烷基,烯基,炔基或氰基甲基,烷基,烯基和炔基各自具有至多5个C原子 及其生理上可接受的盐,表现出血压,心肌收缩和抗溃疡活性。
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公开(公告)号:US3980797A
公开(公告)日:1976-09-14
申请号:US586808
申请日:1975-06-13
IPC分类号: C07D487/04
CPC分类号: C07D487/04
摘要: Hexahydro-diazepino-indoles of the formula ##SPC1##Wherein R.sup.1 is H, F, Cl, CF.sub.3, alkyl or alkoxy each of 1 to 3 carbon atoms; R.sup.2 is H, alkyl or cycloalkyl or alkenyl each of up to 6 carbon atoms, or alkyl of up to 6 carbon atoms substituted by oxo oxygen and/or amino or alkylated amino of 2 to 6 carbon atoms and/or aryl of 6 to 8 carbon atoms; and Z is 0 or (H,H), and physiologically acceptable acid addition salts thereof, possess CNS depressant activity.
摘要翻译: 式WHERE R1的六氢 - 二氮杂吲哚 - 吲哚是1至3个碳原子的H,F,Cl,CF 3,烷基或烷氧基; R2是H,烷基或环烷基或各自具有至多6个碳原子的链烯基,或由氧代氧和/或2至6个碳原子的氨基或烷基化氨基取代的至多6个碳原子的烷基和/或6至8的芳基 碳原子 并且Z为0或(H,H)及其生理上可接受的酸加成盐,具有CNS抑制活性。
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公开(公告)号:US4916128A
公开(公告)日:1990-04-10
申请号:US202294
申请日:1988-06-06
IPC分类号: A61K31/54 , A61K31/55 , A61P7/02 , A61P9/00 , A61P9/08 , C07D417/04 , C07D417/14
CPC分类号: C07D417/04 , C07D417/14
摘要: Thiadiazinones of the formula I ##STR1## wherein A is --CHR.sup.4 --CHR.sup.5 --, --CH.sub.2 --CR.sup.4 R.sup.5 --, --CR.sup.4 R.sup.5 --CH.sub.2 --, --CHR.sup.4 --CHR.sup.5 --CH.sub.2 --, --CHR.sup.4 --CH.sub.2 --CHR.sup.5 --, --CH.sub.2 --CHR.sup.4 --CHR.sup.5 --, --CR.sup.4 R.sup.5 --CH.sub.2 CH.sub.2 --, --CH.sub.2 --CR.sup.4 R.sup.5 --CH.sub.2 -- or --CH.sub.2 CH.sub.2 --CR.sup.4 R.sup.5 --,R.sup.1, R.sup.2, R.sup.3, R.sup.4 and R.sup.5 are each independently H, C.sub.1-5 -alkyl, C.sub.2-5 -alkenyl or C.sub.2-5 -alkinyl,R.sup.3 is also C.sub.1-15 -acyl,R.sup.6 is H, alkyl, alkoxyl, OH, F, Cl, Br or I andZ is (H, H), (H, alkyl), (alkyl, alkyl) or O,the alkyl, alkenyl, alkinyl and/or alkoxy groups in each case containing up to 5 C atoms, but wherein, if A is --CH.sub.2 CH.sub.2 -- and Z is O, one of the radicals R.sup.1, R.sup.2, R.sup.3 and R.sup.6 must be other than H,and salts thereof demonstrate positive inotropic action and are suitable for combating cardiovascular diseases.
摘要翻译: 其中A是-CHR 4 -CHR 5 - , - CH 2 - CR 4 R 5 - , - CR 4 R 5 -CH 2 - , - CHR 4 -CHR 5 -CH 2 - , - CHR 4 -CH 2 - CHR 5 - , - CH 2 CHR 4 - CHR5-,-CR4R5-CH2CH2-,-CH2-CR4R5-CH2-或-CH2CH2-CR4R5-,R1,R2,R3,R4和R5各自独立地为H,C1-5烷基,C2-5-烯基或C2 -5-炔基,R 3还为C 1-15酰基,R 6为H,烷基,烷氧基,OH,F,Cl,Br或I,Z为(H,H),(H,烷基) )或O,每种情况下的烷基,烯基,炔基和/或烷氧基含有至多5个C原子,但其中,如果A是-CH 2 CH 2 - 并且Z是O,基团R 1,R 2,R 3和R 6中的一个 必须不是H,其盐表现出正性肌力作用,并且适用于对抗心血管疾病。
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