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    • 4. 发明授权
    • Cyclic diamine derivatives
    • 环二胺衍生物
    • US4115569A
    • 1978-09-19
    • US606488
    • 1975-08-21
    • Rolf-Ortwin WeberAlfons SoderIstvan Boksay
    • Rolf-Ortwin WeberAlfons SoderIstvan Boksay
    • A61K31/495C07D405/06C07D409/14C07D295/10
    • C07D409/14A61K31/495C07D405/06
    • A compound having the general formula or an acid addition salt thereof ##STR1## in which formula R.sub.1 is selected from the group consisting ofA. an at least mononuclear heterocyclic group having 4 to 10 carbon atoms in the ring system bound to the group ##STR2## through a carbon atom and containing at least one oxygen, nitrogen or sulphur atom,B. substitution products of (A) containing at least one substituent selected from the group consisting of halogen, trifluoromethyl, hydroxy, alkoxy of 1 to 3 carbon atoms, unsubstituted amino, amino substituted by up to two alkyl groups each having 1 to 3 carbon atoms and alkyl groups having 1 to 6 carbon atoms,X is oxygen, sulphur or an NH-group,Y is an alkylene group having 1 to 3 carbon atoms in the chain, or an alkylene group having 1 to 3 carbon atoms in the chain substituted by (a) up to 3 alkyl groups each having up to 3 carbon atoms and a total of not more than 8 carbon atoms, or (b) substituted by one or two phenyl groups,R.sub.2 is selected from the group consisting ofC. an at least mononuclear carbocyclic or heterocyclic group having 4 to 10 carbon atoms in the ring system, containing but one heteroatom in a ring,D. substitution products of (C) containing at least one substituent selected from the group consisting of nitro, halogen, trifluoromethyl, alkyl having 1 to 6 carbon atoms, hydroxy, alkoxy having 1 to 3 carbon atoms, unsubstituted amino groups and amino groups substituted by up to two alkyl groups each having 1 to 3 carbon atoms,R.sub.3 is hydrogen or up to two substituents selected from alkyl groups having up to 2 carbon atoms and phenyl groups.n is 2 or 3;A process for its preparation and a pharmaceutical composition containing said compound (I).
    • 具有通式的化合物或其酸加成盐,其中式R1选自A.在环系中结合有至少单个的具有4至10个碳原子的单核杂环基 含有至少一个氧原子,氮原子或硫原子的基团“IMAGE”,B.含有至少一个选自卤素,三氟甲基,羟基,1〜3的烷氧基的取代基的(A) 碳原子,未取代的氨基,被至多两个各自具有1至3个碳原子的烷基和具有1至6个碳原子的烷基取代的氨基,X是氧,硫或NH-基,Y是具有1至 该链中的3个碳原子或链中具有1至3个碳原子的亚烷基被(a)至多3个各自具有至多3个碳原子和总共不超过8个碳原子的烷基取代,或( b)被一个或两个苯基取代,R2是sele 在环系中具有4-10个碳原子的至少单核碳环或杂环基团,在环中含有一个杂原子,D.含有至少一个选自以下的取代基的取代产物:(C) 由硝基,卤素,三氟甲基,具有1至6个碳原子的烷基,羟基,具有1至3个碳原子的烷氧基,未取代的氨基和被至多两个各自具有1至3个碳原子的烷基取代的氨基,R3, 是氢或至多两个选自具有至多2个碳原子的烷基和苯基的取代基。
    • 5. 发明授权
    • Phosphinyl compounds
    • 磷化合物
    • US4091095A
    • 1978-05-23
    • US702604
    • 1976-07-06
    • Alfons SoderKlaus Perrey
    • Alfons SoderKlaus Perrey
    • C07F9/53C07F9/58A61K31/66C07C101/50
    • C07F9/582C07F9/5304
    • A phosphinyl derivative of formula ##STR1## wherein X is selected from the group consisting of a carbon atom with a hydrogen atom attached thereto and a nitrogen atom,R.sup.1 isA. a phenyl radical,B. a quinolyl radical,C. one of the radicals (a) and (b) being substituted by at least one substituent selected from the group consisting of halogen, trifluoromethyl and 1 to 3 alkyl radicals having in total up to 4 carbon atoms,R.sup.2 is selected from the group consisting of a dialkylphosphinylalkyl radical and a dialkyl phosphinyl-hydroxyalkyl radical each of said radicals R.sup.2 having a total of from 3 to 7 carbon atomsAnd acid addition salts thereof, pharmaceutical preparations containing said derivatives.
    • 式其中X选自具有与其连接的氢原子的碳原子和氮原子,式为“IMAGE”的氧膦基衍生物,R1为A.苯基放射性,B.喹啉衍生物,C. (A)和(B)由至少一个由卤素,三氟甲磺酸和1至3个碱基组成的组选择的一个取代基取代,其具有总计4个碳原子,R2选自二烷基氧膦基烷基 和二烷基氧膦基 - 羟烷基,每个所述基团R 2具有总共3至7个碳原子和其酸加成盐,含有所述衍生物的药物制剂。
    • 7. 发明授权
    • Cyclic diamine derivatives
    • 环二胺衍生物
    • US4374990A
    • 1983-02-22
    • US88338
    • 1979-10-26
    • Rolf-Ortwin WeberAlfons SoderIstvan Boksay
    • Rolf-Ortwin WeberAlfons SoderIstvan Boksay
    • C07D209/42A61K31/495A61K31/55A61P9/08A61P25/04A61P25/18A61P25/24A61P25/26A61P29/00A61P31/04C07D209/50C07D213/74C07D213/81C07D213/82C07D215/04C07D215/12C07D307/54C07D307/68C07D307/81C07D307/82C07D307/85C07D309/08C07D309/28C07D311/04C07D311/22C07D311/58C07D333/20C07D333/38C07D403/06C07D405/06C07D405/12C07D407/12C07D409/06C07D409/12C07D409/14C07D405/02
    • C07D405/06A61K31/495C07D409/14Y10S514/906
    • A compound having the general formula or an acid addition salt thereof ##STR1## in which formula R.sub.1 is selected from the group consisting of(A) an at least mononuclear heterocyclic group having 4 to 10 carbon atoms in the ring system bound to the group ##STR2## through a carbon atom and containing at least one oxygen, nitrogen or sulphur atom,(B) substitution products of (A) containing at least one substituent selected from the group consisting of halogen, trifluoromethyl, hydroxy, alkoxy of 1 to 3 carbon atoms, unsubstituted amino, amino substituted by up to two alkyl groups each having 1 to 3 carbon atoms and alkyl groups having 1 to 6 carbon atoms,X is oxygen, sulphur or an NH-group,Y is an alkylene group having 1 to 3 carbon atoms in the chain, or an alkylene group having 1 to 3 carbon atoms in the chain substituted by (a) up to 3 alkyl groups each having up to 3 carbon atoms and a total of not more than 8 carbon atoms, or (b) substituted by one or two phenyl groups,R.sub.2 is selected from the group consisting of(c) an at least mononuclear carbocyclic or heterocyclic group having 4 to 10 carbon atoms in the ring system, containing but one heteroatom in a ring,(D) substitution products of (C) containing at least one substituent selected from the group consisting of nitro, halogen, trifluoromethyl, alkyl having 1 to 6 carbon atoms, hydroxy, alkoxy having 1 to 3 carbon atoms, unsubstituted amino groups and amino groups substituted by up to two alkyl groups each having 1 to 3 carbon atoms,R.sub.3 is hydrogen or up to two substituents selected from alkyl groups having up to 2 carbon atoms and phenyl groups. n is 2 or 3; a process for its preparation and a pharmaceutical composition containing said compound (I).
    • 具有通式的化合物或其酸加成盐,其中式R 1选自(A)环系中具有4至10个碳原子的至少单核杂环基,其结合到 通过碳原子并含有至少一个氧,氮或硫原子的基团,(B)含有至少一个选自卤素,三氟甲基,羟基,烷氧基的取代基的(A)的取代产物1 至3个碳原子,未取代的氨基,被至多两个各自具有1至3个碳原子的烷基和具有1至6个碳原子的烷基取代的氨基,X是氧,硫或NH-基,Y是具有 链中有1至3个碳原子,或链中具有1至3个碳原子的亚烷基被(a)最多3个具有多达3个碳原子的烷基和总共不超过8个碳原子的烷基取代, 或(b)被一个或两个苯基取代,R 2是se 由(c)环系中具有4至10个碳原子的至少单核碳环或杂环基团组成的基团,其在环中含有一个杂原子;(D)含有至少一个取代基的(C)取代产物 选自硝基,卤素,三氟甲基,具有1至6个碳原子的烷基,羟基,具有1至3个碳原子的烷氧基,未取代的氨基和被至多两个各自具有1至3个碳原子的烷基取代的氨基。 ,R 3是氢或至多两个选自具有至多2个碳原子的烷基和苯基的取代基。