会员体验
专利管家(专利管理)
工作空间(专利管理)
风险监控(情报监控)
数据分析(专利分析)
侵权分析(诉讼无效)
联系我们
交流群
官方交流:
QQ群: 891211   
微信请扫码    >>>
现在联系顾问~
热词
    • 2. 发明公开
    • N-/Arylethyl/-N-alkyl-2-(1-pyrrolidinyl)ethylamine derivatives for CNS disorders
    • N-(甲苯基乙基)-N-烷基-2-(1-吡咯烷基)乙胺,用于Erkrankungen des ZN-Systems。
    • EP0518216A2
    • 1992-12-16
    • EP92109470.2
    • 1992-06-04
    • G.D. Searle & Co.
    • De Costa, Brian R.Radesca, LilianBowen, WayneLong, JosephWalker, J. MichaelRice, Kenneth C.Gray, Nancy M.Contreras, Patricia C.
    • C07D295/12A61K31/395
    • C07D295/13
    • Certain N-[arylethyl]-N-alkyl-2-(1-pyrrolidinyl)ethylamine compounds are described for treatment of CNS disorders such as cerebral ischemia, psychotic disorders, convulsions and parkinsonism. Compounds of particular interest are of the formula

      wherein R 1 is selected from hydrido, loweralkyl, cycloalkylalkyl of four to six carbon atoms and loweralkenylloweralkyl; wherein each of R 2 and R 3 is independently selected from hydrido and loweralkyl; wherein each of R 4 through R 9 is independently selected from hydrido, hydroxy, loweralkyl, benzyl, phenoxy, benzyloxy and haloloweralkyl; wherein m is a number selected from one through three; wherein n is a number selected from four through seven; wherein p is a number selected from zero through four; wherein A is selected from phenyl, naphthyl and thienyl; wherein any of the foregoing A groups can be further substituted with one or more substituents independently selected from hydrido, hydroxy, loweralkyl, loweralkoxy, halo, haloloweralkyl, amino, monoloweralkylamino and diloweralkylamino; or a pharmaceutically acceptable salt thereof.
    • 描述了某些N- [芳基乙基] -N-烷基-2-(1-吡咯烷基)乙胺化合物用于治疗中枢神经系统疾病如脑缺血,精神障碍,抽搐和帕金森综合征。 特别感兴趣的化合物具有式CHEM,其中R 1选自4至6个碳原子的氢,低级烷基,环烷基烷基和低级链烯基低级烷基; 其中R 2和R 3各自独立地选自氢和低级烷基; 其中R 4至R 9各自独立地选自氢,羟基,低级烷基,苄基,苯氧基,苄氧基和卤代低级烷基; 其中m是选自1至3的数; 其中n是选自四至七的数字; 其中p是选自0至4的数字; 其中A选自苯基,萘基和噻吩基; 其中前述A基团中的任一个可以进一步被一个或多个独立地选自氢,羟基,低级烷基,低级烷氧基,卤素,卤代低级烷基,氨基,单低级烷基氨基和二低级烷基氨基的取代基取代。 或其药学上可接受的盐。
    • 4. 发明公开
    • Ethanobicyclic amine derivatives for CNS disorders
    • Ethanobicyclische AminderivatefürCNS-Erkrankungen。
    • EP0455195A2
    • 1991-11-06
    • EP91106922.7
    • 1991-04-29
    • G.D. Searle & Co.
    • Gray, Nancy M.Cheng, Brian K.
    • C07D295/033C07D295/03A61K31/445A61K31/435C07D295/02
    • C07D295/033C07C2603/68C07C2603/72
    • Certain ethanobicyclic amine compounds are described for treatment of CNS disorders such as psychotic disorders, convulsions, dystonia and cerebral ischemia. Compounds of particular interest are of the formula

      wherein each of R¹, R², R³, R⁴, Y and Z is independently selected from hydrido, hydroxy, alkyl, cycloalkyl, cycloalkylalkyl, phenalkyl, phenyl, alkoxy, phenoxy, phenalkoxy, alkoxyalkyl, halo, haloalkyl and hydroxyalkyl; wherein R³ and R⁴ may be taken together to form oxo;
      wherein each of R⁵, R⁶, R⁷, R⁸, R⁹ and R¹⁰ is independently selected from hydrido, alkyl, cycloalkyl, hydroxyalkyl, fluoroalkyl, cycloalkylalkyl, alkoxyalkyl, phenalkyl and phenyl; wherein G within the nitrogen-containing cyclohetero moiety is selected from

      wherein R¹¹ is selected from hydrido, alkyl, cycloalkyl, cycloalkylalkyl, phenyl, phenalkyl, alkoxyalkyl and hydroxyalkyl; wherein each of R¹² and R¹³ is independently selected from hydrido, hydroxy, alkyl, phenalkyl, phenyl, alkoxy, fluoroalkyl and fluoro; wherein m is one or two; wherein p is a number selected from zero through four, inclusive; wherein each of q and r is a number independently selected from one through three, inclusive, with the proviso that sum of q and r is a number from three through six, inclusive; with the further proviso that the nitrogen-containing cyclohetero moiety must be attached at one position selected from R³, R⁴, ring-position two, and ring-position three; or the pharmaceutically-acceptable salts thereof.
    • 描述了某些乙酰胆碱胺化合物用于治疗中枢神经系统疾病如精神病,抽搐,肌张力障碍和脑缺血。 特别感兴趣的化合物具有式CHEM,其中R 1,R 2,R 3,R 4,Y和Z各自独立地选自氢,羟基,烷基,环烷基,环烷基烷基 ,苯烷基,苯基,烷氧基,苯氧基,苯烷氧基,烷氧基烷基,卤素,卤代烷基和羟烷基; 其中R 3和R 4可以一起形成氧代; 其中R 5,R 6,R 7,R 8,R 9和R 10各自独立地选自氢,烷基,环烷基,羟基烷基,氟代烷基,环烷基烷基 ,烷氧基烷基,苯烷基和苯基; 其中含氮环杂环部分中的G选自CHEM,其中R 1选自氢,烷基,环烷基,环烷基烷基,苯基,苯烷基,烷氧基烷基和羟烷基; 其中R 1和R 2各自独立地选自氢,羟基,烷基,苯烷基,苯基,烷氧基,氟烷基和氟; 其中m是一个或两个; 其中p是选自0至4的数字(包括端值); 其中q和r各自独立地选自一至三个,其中q和r之和是三至六的数,包括端值在内; 进一步的条件是含氮环杂环部分必须连接在选自R 3,R 4,环位置2和环3位的一个位置; 或其药学上可接受的盐。
    • 5. 发明公开
    • Propanobicyclic amine derivatives for CNS disorders
    • Propanbicyclische aminderivatefürZNSFunktionsstörungen。
    • EP0449301A1
    • 1991-10-02
    • EP91105041.7
    • 1991-03-28
    • G.D. Searle & Co.
    • Gray, Nancy M.Cheng, Brian K.
    • C07D295/033C07D295/096C07C211/38C07C211/42A61K31/135A61K31/495
    • C07D295/088C07C211/42C07C2603/78C07D295/03C07D295/033
    • Certain propanobicyclic amine compounds are described for treatment of CNS disorders such as psychotic disorders, convulsions, dystonia and cerebral ischemia. Compounds of particular interest are of the formula


      wherein each of R 1 , R 2 , R 3 , R 4 , Y and Z is independently selected from hydrido, hydroxy, alkyl, cycloalkyl, cycloalkylalkyl, phenalkyl, phenyl, alkoxy, phenoxy, phenalkoxy, alkoxyalkyl, halo, haloalkyl and hydroxyalkyl; wherein R 3 and R 4 may be taken together to form oxo;
      wherein each of R 9 , R 10 , R", R 12 , R 13 and R 14 is independently selected from hydrido, alkyl, cycloalkyl, hydroxyalkyl, fluoroalkyl, cycloalkylalkyl, alkoxyalkyl, phenalkyl and phenyl; wherein G within the nitrogen-containing cyclohetero moiety is selected from

      wherein R 15 is selected from hydrido, alkyl, cycloalkyl, cycloalkylalkyl, phenyl, phenalkyl, alkoxyalkyl and hydroxyalkyl; wherein each of R 16 and R17 is independently selected from hydrido, hydroxy, alkyl, phenalkyl, phenyl, alkoxy, fluoroalkyl and fluoro; wherein m is one or two; wherein p is a number selected from zero through four, inclusive; wherein each of q and r is a number independently selected from one through three, inclusive, with the proviso that sum of q and r is a number from three through six, inclusive; with the further proviso that the nitrogen-containing cyclohetero moiety must be attached at one position selected from R 3 , R 4 , ring-position two, ring-position three and ring-position four; or the pharmaceutically-acceptable salts thereof.
    • 描述了某些丙三醇胺化合物用于治疗中枢神经系统疾病如精神病,抽搐,肌张力障碍和脑缺血。 特别感兴趣的化合物具有式CHEM,其中R 1,R 2,R 3,R 4,Y和Z各自独立地选自氢,羟基,烷基,环烷基,环烷基烷基 ,苯烷基,苯基,烷氧基,苯氧基,苯烷氧基,烷氧基烷基,卤素,卤代烷基和羟烷基; 其中R 3和R 4可以一起形成氧代; 其中R 9,R 1,R 1,R 1,R 2,R 3和R 4各自独立地选自 烷基,环烷基,羟基烷基,氟烷基,环烷基烷基,烷氧基烷基,苯烷基和苯基; 其中含氮环杂环部分中的G选自CHEM,其中R 1 5选自氢化,烷基,环烷基,环烷基烷基,苯基,苯烷基,烷氧基烷基和羟烷基; 其中R 1和R 6各自独立地选自氢,羟基,烷基,苯烷基,苯基,烷氧基,氟烷基和氟; 其中m是一个或两个; 其中p是选自0至4的数字(包括端值); 其中q和r各自独立地选自一至三个,其中q和r之和是三至六的数,包括端值在内; 进一步的条件是含氮环杂环部分必须连接在选自R 3,R 4,环位2,环3位和环4位的一个位置上; 或其药学上可接受的盐。
    • 6. 发明公开
    • N-(1-thienylcycloalkyl)alkenylamines for treatment of neurotoxic injury
    • N-(1-噻吩基环烷基)烯基胺zur Behandlung von neurotoxischen Krankheiten。
    • EP0317953A2
    • 1989-05-31
    • EP88119410.4
    • 1988-11-22
    • G.D. Searle & Co.
    • Rice, Kenner C.Jacobson, Arthur E.Thurkauf, AndrewMattson, Mariena V.O'Donohue, Thomas L.Contreras, Patricia C.Gray, Nancy M.
    • C07D333/20C07D409/06A61K31/38A61K31/44
    • C07D409/06C07D333/20
    • Compounds, compositions and methods of treatment are described to control brain damage associated with anoxia or ischemia which typically follows stroke, cardiac arrest or perinatal asphyxia. The treatment includes administration of an N-(1-thienylcycloalkyl)alkenylamine compound as an antagonist to inhibit excitotoxic actions at major neuronal excitatory amino acid receptor sites. Compounds of most interest are those of the formula
      wherein R¹ is one or more groups selected from hydrido, alkyl of one to about five carbon atoms, cycloalkyl of three to about five carbon atoms, alkenyl of two to about five carbon atoms, hydroxyl and alkoxy; wherein each of R² is one or more groups selected from hydrido, alkyl of one to about five carbon atoms, cycloalkyl of three to about five carbon atoms, alkenyl of two to about five carbon atoms, hydroxyl, oxo and alkoxy; wherein R⁵ is one or more groups selected from hydrido, alkyl of one to about five carbon atoms, cycloalkyl of three to about five carbon atoms, alkenyl of two to about five carbon atoms, hydroxyl and alkoxy; and wherein the broken line within the N-containing ring represents a double bond between any two adjacent carbon atoms involving the 3-, 4- and 5-positions of the N-containing ring.
    • 描述了治疗的化合物,组合物和方法以控制与缺氧或缺血相关的脑损伤,其通常在中风,心脏骤停或围产期窒息之后。 该治疗包括施用N-(1-噻吩基环烷基)链烯基胺化合物作为拮抗剂以抑制主要神经元兴奋性氨基酸受体位点的兴奋性毒性作用。 最感兴趣的化合物是式CHEM的化合物,其中R 1是一个或多个选自氢化物,1至约5个碳原子的烷基,3至约5个碳原子的环烷基,2至约5个的烯基 碳原子,羟基和烷氧基; 其中R 2为选自氢化物,1至约5个碳原子的烷基,3至约5个碳原子的环烷基,2至约5个碳原子的链烯基,羟基,氧代和烷氧基的一个或多个基团; 其中R 5为一个或多个选自氢化物,一至约五个碳原子的烷基,三至五个碳原子的环烷基,二至五个碳原子的烯基,羟基和烷氧基; 并且其中所述含N环的虚线表示涉及所述含N环的3-,4-和5-位的任何两个相邻碳原子之间的双键。
    • 8. 发明公开
    • Dihetero nitrogen-containing cycloheteroethanoanthracene derivatives as antipsychotic agents
    • 含有氮氧化物的环十二烷基衍生物作为抗生素代谢物
    • EP0405436A3
    • 1992-02-26
    • EP90112113.7
    • 1990-06-26
    • G.D. Searle & Co.
    • Gray, Nancy M.
    • C07D295/033C07D295/088C07D295/182C07D239/42C07D487/04A61K31/495
    • C07D239/42C07C2603/88C07D295/03C07D295/088C07D295/185C07D487/04
    • A class of ethanoanthracene derivatives is described having use in treatment of CNS disorders such as psychotic, convulsive and dystonic disorders. Compounds of particular interest are those of the formula
      wherein each of R 5 and R 6 is independently selected from hydrido, loweralkyl, benzyl and phenyl; wherein each of R 7 through R 11 - is independently selected from hydrido, loweralkyl, hydroxy, benzyl, phenyl, loweralkoxy, phenoxy, benzyloxy, halo and haloloweralkyl; wherein R 12 may be selected from hydrido, loweralkyl, cycloalkyl of five or six carbon atoms, cycloalkylalkyl of six or seven carbon atoms, phenyl, hydroxyloweralkyl, and heteroaryl selected from saturated or fully unsaturated heterocyclic rings containing five to seven ring members of which one or two ring members are nitrogen atom; wherein each Y is independently one or more groups selected from hydrido, hydroxy, loweralkyl, benzyl, phenyl, loweralkoxy, phenoxy, haloloweralkyl, halo, and loweralkanoyl; and wherein each of R 13 through R 20 is independently selected from hydrido, lower alkyl, benzyl, phenyl and halo; wherein R 12 together with one of R 13 , R 14 , R 19 or R 20 may form a fused heterocyclic ring containing five or six ring members; or a pharmaceutically-acceptable salt thereof.
    • 描述了一类用于治疗中枢神经系统疾病如精神病性,惊厥性和肌张力障碍性疾病的乙酰胆碱衍生物。 特别感兴趣的化合物是式CHEM的化合物,其中R 5和R 6各自独立地选自氢,低级烷基,苄基和苯基; 其中R 7至R 1中的每一个独立地选自氢,低级烷基,羟基,苄基,苯基,低级烷氧基,苯氧基,苄氧基,卤代和卤代低级烷基; 其中R 1可以选自氢或低级烷基,5或6个碳原子的环烷基,6或7个碳原子的环烷基烷基,苯基,羟基低级烷基和选自饱和或完全不饱和的杂环的杂芳基, 一个或两个环成员为氮原子的环成员; 其中每个Y独立地是一个或多个选自氢,羟基,低级烷基,苄基,苯基,低级烷氧基,苯氧基,卤代低级烷基,卤素和低级烷酰基的基团。 并且其中R 1至3“至R 2”各自独立地选自氢,低级烷基,苄基,苯基和卤素; 其中R 1与R 1,R 3,R“4”,R“9”或R 2“中的一个一起形成稠合杂环,其含有 五六个戒指成员; 或其药学上可接受的盐。
    • 10. 发明公开
    • 1,2-diarylethylamines for treatment of neurotoxic injury
    • 1,2-Diarylethylamine zur Behandlung neurotoxischer Verletzungen。
    • EP0346791A1
    • 1989-12-20
    • EP89110572.8
    • 1989-06-12
    • G.D. Searle & Co.
    • Gray, Nancy M.Cheng, Brian K.
    • C07D295/00C07D211/70C07D211/14C07D333/20C07D307/36A61K31/395
    • C07D295/03C07D213/38C07D295/073C07D295/092C07D295/096C07D295/104C07D307/52C07D333/20C07D409/06
    • Compounds, compositions and methods of treatment are described to control brain damage associated with anoxia or ischemia which typically follows stroke, cardiac arrest or perinatal asphyxia. The treatment includes administration of a 1,2-diarylethylamine compound as an antagonist to inhibit excitotoxic actions at major neuronal excitatory amino acid receptor sites. Compounds of interest are those of the formula
      wherein each of R¹ and R² is a group independently selected from hydrido, alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkenyl, cycloalkynyl, hydroxyl, alkoxy, halo, cyano, nitro and mercapto, or wherein R¹ and R² may be taken together to form an oxo group or to form a saturated or partially unsaturated carbocyclic group having three to eight ring carbons; wherein each of Ar¹ and Ar² is a group independently selected from aryl and heteroaryl having one or two heteroatoms selected from N, O and S; and wherein any of the foregoing Ar¹ and Ar² groups having a substitutable position msy be substituted with one or more radicals selected from hydrido, alkyl, cycloalkyl, halo, haloalkyl, alkenyl, alkynyl, hydroxyl, hydroxyalkyl, alkoxy, alkoxyalkyl, amino, cyano, nitro and mercapto; wherein X is selected from CH, CH₂, NH, O and S, to form a ring having five to eight members provided that such ring is saturated or contains one double bond or is benzo-fused; and wherein Y is one or more a groups selected from hydrido, alkyl, cycloalkyl, halo, haloalkyl, alkenyl, alkynyl, hydroxyl, hydroxy­alkyl, alkoxy, alkoxyalkyl, amino, cyano, nitro and mercapto; or a pharmaceutically acceptable salt thereof.
    • 描述了治疗的化合物,组合物和方法以控制与缺氧或缺血相关的脑损伤,其通常在中风,心脏骤停或围产期窒息之后。 该治疗包括施用1,2-二氨基乙胺化合物作为拮抗剂以抑制主要神经元兴奋性氨基酸受体位点的兴奋性毒性作用。 感兴趣的化合物是式CHEM的化合物,其中R 1和R 2各自独立地选自氢,烷基,烯基,炔基,环烷基,环烯基,环炔基,羟基,烷氧基,卤素,氰基 ,硝基和巯基,或其中R 1和R 2可以一起形成氧代基或形成具有3-8个环碳的饱和或部分不饱和的碳环基; 其中Ar 1和Ar 2各自独立地选自具有一个或两个选自N,O和S的杂原子的芳基和杂芳基; 并且其中具有可取代位置的任何上述Ar 1和Ar 2基团被一个或多个选自氢,烷基,环烷基,卤素,卤代烷基,烯基,炔基,羟基,羟烷基,烷氧基, 烷氧基烷基,氨基,氰基,硝基和巯基; 其中X选自CH,CH 2,NH,O和S,以形成具有5至8个成员的环,条件是该环为饱和或含有一个双键或苯并稠合; 烷基,环烷基,卤素,卤代烷基,烯基,炔基,羟基,羟基烷基,烷氧基,烷氧基烷基,氨基,氰基,硝基和巯基中的一个或多个基团。 或其药学上可接受的盐。