-
公开(公告)号:US4870085A
公开(公告)日:1989-09-26
申请号:US175066
申请日:1988-03-30
申请人: Thomas Glaser , Siegfried Raddatz , Jorg Traber , Allen, George
发明人: Thomas Glaser , Siegfried Raddatz , Jorg Traber , Allen, George
IPC分类号: A61K31/40 , A61K31/4427 , A61K31/445 , A61P9/06 , A61P9/10 , A61P25/20 , A61P43/00 , C07D209/16 , C07D401/06 , C07D403/06
CPC分类号: C07D401/06 , C07D209/16
摘要: Novel tryptamines of the formula ##STR1## in which X is an alkylene chain or 2 to 4 carbon atoms wherein a carbon atom may be replaced by O or N-lower alkyl, and wherein a carbon atoms may be substituted by lower alkyl,R is hydrogen, lower alkyl, lower alkoxy, phenyl-lower alkyl, phenyl-lower alkoxy, hydroxy, amino-lower alkyl, fluorine, chlorine, bromine, cyano, carbamoyl or azido,R.sup.1, R.sup.2, R.sup.3 and R.sup.4 each independently is hydrogen or lower alkyl,R.sup.5 is hydrogen, R.sup.6 --CO-- or R.sup.6 --SO.sub.2 --, andR.sup.6 is amino, lower alkoxy, phenyl or lower alkyl-phenyl,or dimers or salts thereof, are effective in treating disorders of the central nervous system.
摘要翻译: 其中X是亚烷基链或2至4个碳原子的式(IMAGE)的新型色胺,其中碳原子可被O或N-低级烷基取代,并且其中碳原子可以被低级烷基取代,R是 氢,低级烷基,低级烷氧基,苯基 - 低级烷基,苯基 - 低级烷氧基,羟基,氨基 - 低级烷基,氟,氯,溴,氰基,氨基甲酰基或叠氮基,R1,R2,R3和R4各自独立地为氢或低级 烷基,R5是氢,R6-CO-或R6-SO2-,R6是氨基,低级烷氧基,苯基或低级烷基 - 苯基,或其二聚体或其盐在治疗中枢神经系统疾病中是有效的。
-
2.
公开(公告)号:US5137901A
公开(公告)日:1992-08-11
申请号:US412694
申请日:1989-09-26
申请人: Bodo Junge , Rudolf Schohe , Peter-Rudolf Seidel , Thomas Glaser , Jorg Traber , Ulrich Benz , Teunis Schuurman , Jean-Marie V. De Vry
发明人: Bodo Junge , Rudolf Schohe , Peter-Rudolf Seidel , Thomas Glaser , Jorg Traber , Ulrich Benz , Teunis Schuurman , Jean-Marie V. De Vry
IPC分类号: A61K31/135 , A61K31/00 , A61K31/165 , A61K31/19 , A61K31/215 , A61K31/35 , A61K31/352 , A61K31/425 , A61K31/428 , A61K31/44 , A61K31/4402 , A61K31/4425 , A61K31/443 , A61K31/47 , A61K31/505 , A61K31/54 , A61K31/5415 , A61P1/00 , A61P5/24 , A61P9/00 , A61P25/20 , A61P25/28 , A61P43/00 , B01J31/14 , C07B61/00 , C07C67/00 , C07C201/00 , C07C205/36 , C07C209/00 , C07C209/08 , C07C209/16 , C07C209/24 , C07C209/42 , C07C209/48 , C07C209/50 , C07C209/60 , C07C211/30 , C07C217/58 , C07C229/14 , C07C233/36 , C07C233/78 , C07C237/04 , C07C237/06 , C07C255/24 , C07C271/20 , C07C311/18 , C07C323/65 , C07D213/75 , C07D213/76 , C07D221/20 , C07D275/06 , C07D285/24 , C07D311/58 , C07D311/64 , C07D311/66 , C07D311/92 , C07D405/12 , C07D417/12 , C07D417/14 , C07D471/10
CPC分类号: C07D213/76 , C07C233/78 , C07C271/20 , C07C311/18 , C07D275/06 , C07D285/24 , C07D311/58 , C07D311/66 , C07D311/92 , C07D405/12 , C07D417/12 , C07D417/14 , C07C2102/10
摘要: For binding 5-HT.sub.1 receptors and thereby treating central nervous system disorders, novel substituted aminomethyltetralins and their heterocyclic analogues of the formula ##STR1## in which Z--denotes a group of the formula ##STR2## R.sup.1, E and F can be hydrogen or other radicals, or salts thereof.
摘要翻译: 对于结合5-HT1受体并因此治疗中枢神经系统疾病,新的取代的氨基甲基四氢萘酮及其式“IMAGE”的其杂环类似物,其中Z代表下式的基团:
R1 ,E和F可以是氢或其它基团,或其盐。 -
公开(公告)号:US5021438A
公开(公告)日:1991-06-04
申请号:US324518
申请日:1989-03-15
申请人: Bodo Junge , Bernd Richter , Thomas Glaser , Jorg Traber
发明人: Bodo Junge , Bernd Richter , Thomas Glaser , Jorg Traber
IPC分类号: A61K31/40 , A61K31/403 , A61K31/425 , A61K31/44 , A61K31/4427 , A61K31/445 , A61K31/495 , A61K31/54 , A61P25/00 , A61P25/24 , A61P25/26 , A61P43/00 , C07D209/90 , C07D401/12 , C07D403/12 , C07D417/12 , C07D521/00
CPC分类号: C07D401/12 , C07D209/90 , C07D417/12
摘要: Novel compounds having an affinity for 5-hydroxytryptamine receptors of the formula ##STR1## in which R.sup.1 stands for H, alkyl, aralkyl or heteroarylalkyl,X stands for H, OCH.sub.3, OH, SCH.sub.3, halogen, CN or CONH.sub.2,Y stands for a straight-chain or branched, saturated or unsaturated alkylene chain having up to 6 carbon atomsandZ stands for a group of the formula ##STR2## --OR.sup.4, --SO.sub.m R.sup.5, --COOR.sup.6 or CONR.sup.7 R.sup.8 or salts thereof.
摘要翻译: 具有式(I)的5-羟基色胺受体的亲和力的新化合物,其中R1代表H,烷基,芳烷基或杂芳基烷基,X代表H,OCH3,OH,SCH3,卤素,CN或CONH2,Y 代表具有至多6个碳原子的直链或支链,饱和或不饱和的亚烷基链,Z代表下式的基团-OR4,-SOmR5,-COOR6或CONR7R8或其盐。
-
公开(公告)号:US5453437A
公开(公告)日:1995-09-26
申请号:US118376
申请日:1993-09-08
申请人: Rudolf Schohe , Peter-Rudolf Seidel , Jorg Traber , Thomas Glaser
发明人: Rudolf Schohe , Peter-Rudolf Seidel , Jorg Traber , Thomas Glaser
IPC分类号: C07D207/12 , C07D207/26 , C07D207/27 , C07D401/06 , C07D403/06 , C07D417/06 , A61K31/40
CPC分类号: C07D207/27 , C07D207/12 , C07D401/06 , C07D403/06 , C07D417/06
摘要: Novel 1,3-disubstituted pyrrolidines active on the central nervous system of the formula ##STR1## wherein A--denotes phenyl or hetaryl, which is optionally fused with aromatic, saturated or unsaturated cyclic or heterocyclic hydrocarbons, where this radical can optionally be substituted,X--denotes --O--CH.sub.2 --, --CH.sub.2 --O-- or --0--,n--denotes a number from 1 to 19, andB--denotes cyano or a group of the formula --COOR.sup.1, --CONR.sup.2 R.sup.3, --SO.sub.2 NR.sup.2 R.sup.3, --SO.sub.m R.sup.4, --NR.sup.5 R.sup.6, or --C.tbd.C--CH.sub.2 --NR.sup.5 R.sup.6,and salts thereof.
摘要翻译: 在式(I)的中枢神经系统上活性的新的1,3-二取代吡咯烷,其中A表示苯基或杂芳基,其任选地与芳族,饱和或不饱和的环状或杂环烃稠合,其中该基团可任选地 被取代,X表示-O-CH 2 - , - CH 2 -O-或-O-,n - 表示1至19的数,B表示氰基或式-COOR 1,-CONR 2 R 3 - SO2NR2R3,-SOmR4,-NR5R6或-C3OND C-CH2-NR5R6,及其盐。
-
公开(公告)号:US5298513A
公开(公告)日:1994-03-29
申请号:US891485
申请日:1992-05-29
申请人: Rudolf Schohe , Thomas Glaser , Jorg Traber , George S. Allen
发明人: Rudolf Schohe , Thomas Glaser , Jorg Traber , George S. Allen
IPC分类号: C07C253/00 , A61K31/135 , A61K31/18 , A61K31/40 , A61K31/435 , A61K31/445 , A61K31/495 , C07C67/00 , C07C227/00 , C07C227/02 , C07C231/00 , C07C233/00 , C07C233/62 , C07C255/58 , C07C271/06 , C07C271/08 , C07C311/00 , C07C311/02 , C07C311/37 , C07C313/00 , C07C317/00 , C07C317/04 , C07C317/14 , C07D209/14 , C07D209/16 , C07D209/44 , C07D209/48 , C07D209/50 , C07D211/26 , C07D211/58 , C07D211/88 , C07D213/82 , C07D275/02 , C07D275/06 , C07D279/02 , C07D285/14 , C07D295/096 , C07D295/10 , C07D453/02 , C07D471/10 , C07D521/00
CPC分类号: C07D209/48 , C07C233/62 , C07C255/00 , C07D209/14 , C07D209/16 , C07D209/44 , C07D211/26 , C07D211/58 , C07D211/88 , C07D213/82 , C07D275/02 , C07D275/06 , C07D279/02 , C07D285/14 , C07D295/096 , C07D453/02 , C07D471/10 , C07C2103/74
摘要: For treatment of disorders of the central nervous system, the cardiovascular system or the intestinal tract, the new substituted basic 2-aminotetralins of the formula ##STR1## in which R.sup.1 represents hydrogen or alkyl,R.sup.2 represents hydrogen, alkyl or acyl, andR.sup.3 represents quinuclidine ora group of the formula --(CH.sub.2).sub.a --R.sup.4, --CH.sub.2 --CH.dbd.CH--(CH.sub.2).sub.b --R.sup.4, --CH.sub.2 --C.tbd.C--(CH.sub.2).sub.b --R.sup.4, ##STR2## wherein a denotes a number from 1 to 10,b denotes a number 0, 1, 2, 3 or 4,c denotes a number 0, 1 or 2,d denotes a number 2 or 3, andX denotes oxygen, sulphur or NR.sup.5,and their salts.
摘要翻译: 为了治疗中枢神经系统,心血管系统或肠道疾病,新的取代的碱式2-氨基四氢萘酚(其中R 1表示氢或烷基,R 2表示氢,烷基或酰基),式(* CHEMICAL STRUCTURE *) 并且R 3表示奎宁环或式 - (CH 2)a -R 4,-CH 2 -CH = CH-(CH 2)b -R 4,-CH 2 -C(三键)C-(CH 2)b -R 4,( *化学结构*)其中a表示1至10的数字,b表示数字0,1,2,3或4,c表示数字0,1或2,d表示数字2或3,X表示 氧,硫或NR5及其盐。
-
公开(公告)号:US5153225A
公开(公告)日:1992-10-06
申请号:US682823
申请日:1991-04-09
申请人: Rudolf Schohe , Thomas Glaser , Jorg Traber , George S. Allen
发明人: Rudolf Schohe , Thomas Glaser , Jorg Traber , George S. Allen
IPC分类号: A61K31/18 , A61K31/445 , C07C233/62 , C07C311/37 , C07D209/14 , C07D209/16 , C07D209/44 , C07D209/48 , C07D211/26 , C07D211/58 , C07D211/88 , C07D213/82 , C07D275/02 , C07D275/06 , C07D279/02 , C07D285/14 , C07D295/096 , C07D453/02 , C07D471/10
CPC分类号: C07D209/48 , C07C233/62 , C07C255/00 , C07D209/14 , C07D209/16 , C07D209/44 , C07D211/26 , C07D211/58 , C07D211/88 , C07D213/82 , C07D275/02 , C07D275/06 , C07D279/02 , C07D285/14 , C07D295/096 , C07D453/02 , C07D471/10 , C07C2103/74
摘要: For treatment of disorders of the central nervous system, the cardiovascular system or the intestinal tract, the new substituted basic 2-aminotetralins of the formula ##STR1## in which R.sup.1 represents hydrogen or alkyl,R.sup.2 represents hydrogen, alkyl or acyl, andR.sup.3 represents quinuclidine or a group of the formula --(CH.sub.2).sub.a --R.sup.4, --CH.sub.2 --CH.dbd.CH--(CH.sub.2).sub.b --R.sup.4, --CH.sub.2 --C.tbd.C--(CH.sub.2).sub.b --R.sup.4, ##STR2## wherein a denotes a number from 1 to 10,b denotes a number 0, 1, 2, 3 or 4,c denotes a number 0, 1 or 2,d denotes a number 2 or 3, andx denotes oxygen, sulphur or NR.sup.5,and their salts.
摘要翻译: 为了治疗中枢神经系统,心血管系统或肠道疾病,新的取代的碱式2-氨基鸟嘌呤,其中R1代表氢或烷基,R2代表氢,烷基或酰基,R3代表式 奎宁环或式 - (CH 2)a -R 4,-CH 2 -CH = CH-(CH 2)b -R 4,-CH 2 -C 3 O C(CH 2)b -R 4,
或 其中a表示1至10的数,b表示数字0,1,2,3或4,c表示数字0,1或2,d表示数字2或3,x表示氧,硫或NR 5 ,及其盐。 -
公开(公告)号:US5026857A
公开(公告)日:1991-06-25
申请号:US378733
申请日:1989-07-12
申请人: Rudolf Schohe , Thomas Glaser , Jorg Traber , George S. Allen
发明人: Rudolf Schohe , Thomas Glaser , Jorg Traber , George S. Allen
IPC分类号: C07C253/00 , A61K31/135 , A61K31/18 , A61K31/40 , A61K31/435 , A61K31/445 , A61K31/495 , C07C67/00 , C07C227/00 , C07C227/02 , C07C231/00 , C07C233/00 , C07C233/62 , C07C255/58 , C07C271/06 , C07C271/08 , C07C311/00 , C07C311/02 , C07C311/37 , C07C313/00 , C07C317/00 , C07C317/04 , C07C317/14 , C07D209/14 , C07D209/16 , C07D209/44 , C07D209/48 , C07D209/50 , C07D211/26 , C07D211/58 , C07D211/88 , C07D213/82 , C07D275/02 , C07D275/06 , C07D279/02 , C07D285/14 , C07D295/096 , C07D295/10 , C07D453/02 , C07D471/10 , C07D521/00
CPC分类号: C07D209/48 , C07C233/62 , C07C255/00 , C07D209/14 , C07D209/16 , C07D209/44 , C07D211/26 , C07D211/58 , C07D211/88 , C07D213/82 , C07D275/02 , C07D275/06 , C07D279/02 , C07D285/14 , C07D295/096 , C07D453/02 , C07D471/10 , C07C2103/74
摘要: For treatment of disorders of the central nervous system, the cardiovascular system or the intestinal tract, the new substituted basic 2-aminotetralins of the formula ##STR1## in which R.sup.1 represents hydrogen or alkyl,R.sup.2 represents hydrogen, alkyl or acyl, andR.sup.3 represents quinuclidine or a group of the formula --(CH.sub.2).sub.a --R.sup.4, --CH.sub.2 --CH.dbd.CH--(CH.sub.2).sub.b --R.sup.4, --CH.sub.2 C.tbd.C--(CH.sub.2).sub.b --R.sup.4, ##STR2## wherein a denotes a number from 1 to 10,b denotes a number 0, 1, 2, 3 or 4,c denotes a number 0, 1 or 2,d denotes a number 2 or 3, andx denotes oxygen, sulphur or NR.sup.5,and their salts.
-
公开(公告)号:US5463105A
公开(公告)日:1995-10-31
申请号:US131267
申请日:1993-10-01
申请人: Rudolf Schohe , Thomas Glaser , Jorg Traber , George S. Allen
发明人: Rudolf Schohe , Thomas Glaser , Jorg Traber , George S. Allen
IPC分类号: C07C253/00 , A61K31/135 , A61K31/18 , A61K31/40 , A61K31/435 , A61K31/445 , A61K31/495 , C07C67/00 , C07C227/00 , C07C227/02 , C07C231/00 , C07C233/00 , C07C233/62 , C07C255/58 , C07C271/06 , C07C271/08 , C07C311/00 , C07C311/02 , C07C311/37 , C07C313/00 , C07C317/00 , C07C317/04 , C07C317/14 , C07D209/14 , C07D209/16 , C07D209/44 , C07D209/48 , C07D209/50 , C07D211/26 , C07D211/58 , C07D211/88 , C07D213/82 , C07D275/02 , C07D275/06 , C07D279/02 , C07D285/14 , C07D295/096 , C07D295/10 , C07D453/02 , C07D471/10 , C07D521/00
CPC分类号: C07D209/48 , C07C233/62 , C07C255/00 , C07D209/14 , C07D209/16 , C07D209/44 , C07D211/26 , C07D211/58 , C07D211/88 , C07D213/82 , C07D275/02 , C07D275/06 , C07D279/02 , C07D285/14 , C07D295/096 , C07D453/02 , C07D471/10 , C07C2103/74
摘要: For treatment of disorders of the central nervous system, the cardiovascular system or the intestinal tract, the new substituted basic 2-aminotetralins of the formula ##STR1## in which R.sup.1 represents hydrogen or alkyl,R.sup.2 represents hydrogen, alkyl or acyl, andR.sup.3 represents quinuclidine or a group of the formula--(CH.sub.2).sub.a --R.sup.4, --CH.sub.2 --CH.dbd.CH--(CH.sub.2).sub.b --R.sup.4, --CH.sub.2 --C.tbd.C--(CH.sub.2).sub.b --R.sup.4, ##STR2## wherein a denotes a number from 1 to 10,b denotes a number 0, 1, 2, 3 or 4,c denotes a number 0, 1 or 2,d denotes a number 2 or 3, andX denotes oxygen, sulphur or NR.sup.5, and their salts.
摘要翻译: 为了治疗中枢神经系统,心血管系统或肠道疾病,新的取代的碱式2-氨基鸟嘌呤,其中R1代表氢或烷基,R2代表氢,烷基或酰基,R3代表式 奎宁环或式 - (CH 2)a -R 4,-CH 2 -CH = CH-(CH 2)b -R 4,-CH 2 -C 3 O C(CH 2)b -R 4,
或 其中a表示1至10的数,b表示数字0,1,2,3或4,c表示数字0,1或2,d表示数字2或3,X表示氧,硫或NR 5 ,及其盐。 -
公开(公告)号:US5037841A
公开(公告)日:1991-08-06
申请号:US336977
申请日:1989-04-12
申请人: Rudolf Schohe , Peter-Rudolf Seidel , Jorg Traber , Thomas Glaser
发明人: Rudolf Schohe , Peter-Rudolf Seidel , Jorg Traber , Thomas Glaser
IPC分类号: A61K31/40 , A61K31/41 , A61K31/425 , A61K31/4427 , A61K31/445 , A61K31/505 , A61K31/54 , A61P25/00 , C07D207/12 , C07D207/26 , C07D207/27 , C07D401/06 , C07D403/06 , C07D417/06
CPC分类号: C07D207/27 , C07D207/12 , C07D401/06 , C07D403/06 , C07D417/06
摘要: Novel 1,3-disubstituted pyrrolidines active on the central nervous system of the formula ##STR1## wherein A denotes phenyl or hetaryl, which is optionally fused with aromatic, saturated or unsaturated cyclic or heterocyclic hydrocarbons, where this radical can optionally be substituted,X denotes --O--CH.sub.2 --, --CH.sub.2 --O-- or --O--,n denotes a number from 1 to 19, andB denotes cyano or a group of the formula --COOR.sup.1, --CONR.sup.2 R.sup.3, --SO.sub.2 NR.sup.2 R.sup.3, --SO.sub.m R.sup.4, --NR.sup.5 R.sup.6, or --C.tbd.C--CH.sub.2 --NR.sup.5 R.sup.6,and salts thereof.
摘要翻译: 在式(I)的中枢神经系统上活性的新的1,3-二取代的吡咯烷,其中A表示苯基或杂芳基,其任选地与芳族,饱和或不饱和的环状或杂环烃稠合,其中该基团可以任选地 X表示-O-CH 2 - , - CH 2 -O-或-O-,n表示1至19的数,B表示氰基或式-COOR 1,-CONR 2 R 3,-SO 2 NR 2 R 3,-SO m R 4 ,-NR5R6或-C3OND C-CH2-NR5R6,及其盐。
-
公开(公告)号:US4937343A
公开(公告)日:1990-06-26
申请号:US247813
申请日:1988-09-22
申请人: Peter-Rudolf Seidel , Harald Horstmann , Jorg Traber , Wolfgang Dompert , Thomas Glaser , Teunis Schuurman
发明人: Peter-Rudolf Seidel , Harald Horstmann , Jorg Traber , Wolfgang Dompert , Thomas Glaser , Teunis Schuurman
IPC分类号: A61K31/505 , A61K31/517 , A61K31/54 , A61P25/00 , A61P25/04 , A61P25/20 , A61P25/24 , A61P25/26 , A61P25/28 , A61P29/00 , C07D239/42 , C07D239/96 , C07D401/12 , C07D403/04 , C07D403/12 , C07D403/14 , C07D417/12
CPC分类号: C07D239/42 , C07D239/96 , C07D401/12 , C07D403/04 , C07D403/12 , C07D403/14 , C07D417/12
摘要: The invention relates to substituted 2-pyrimidinyl-1-piperazine derivatives defined herein by formula (I), processes for their manufacture, compositions containing said substituted 2-pyrimidinyl-1-piperazine derivatives as active materials and the use of said compounds and compositions as agents effecting the central nervous system. Also included in the invention are intermediates of formula (VIII) for making the active formula (I) compounds.
-
-
-
-
-
-
-
-
-