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1. 发明授权

US5130330A Nitrogen-containing cyclohetero cycloalkylaminoaryl derivatives for CNS disorders 失效
标题翻译：用于CNS疾病的含氮环己基氨基胆碱衍生物
公开(公告)号：US5130330A
公开(公告)日：1992-07-14
申请号：US473008
申请日：1990-01-31
申请人： Brian R. de Costa , Kenner C. Rice , Nancy M. Gray , Patricia C. Contreras , Arthur E. Jacobson , Andrew Thurkauf , Lilian A. Radesca , Wayne D. Bowen
发明人： Brian R. de Costa , Kenner C. Rice , Nancy M. Gray , Patricia C. Contreras , Arthur E. Jacobson , Andrew Thurkauf , Lilian A. Radesca , Wayne D. Bowen
IPC分类号： A61K31/40 , A61K31/4025 , A61P25/00 , C07D295/12 , C07D295/135 , C07D405/12
CPC分类号： C07D295/135
摘要： Certain nitrogen-containing cyclohetero cycloalkylaminoaryl compounds are described for treatment of CNS disorders such as cerebral ischemia, psychotic disorders and convulsions. Compounds of particular interest are of the formula ##STR1## wherein R.sup.1 is selected from hydrido, loweralkyl, cycloalkylalkyl of four to six carbon atoms, and loweralkenylloweralkyl; wherein each of R.sup.2 and R.sup.3 is independently selected from hydrido and loweralkyl; wherein each of R.sup.4 through R.sup.7, R.sup.10 and R.sup.11 is independently selected from hydrido, hydroxy, loweralkyl, benzyl, phenoxy, benzyloxy and haloloweralkyl; wherein n is a number selected from four through six; wherein p is a number selected from zero through four; wherein q is a number selected from three through five; 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.
摘要翻译：描述某些含氮环杂环烷基氨基芳基化合物用于治疗中枢神经系统疾病如脑缺血，精神病和惊厥。特别感兴趣的化合物具有下式：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R2和R3各自独立地选自氢和低级烷基; 其中R 4至R 7，R 10和R 11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n是选自四至六的数; 其中p是选自零至四的数字; 其中q是选自三至五的数; 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。

2. 发明授权

US5739158A Nitrogen-containing cyclohetero cycloalkylaminoaryl derivatives for CNS disorders 失效
标题翻译：用于CNS疾病的含氮环杂环烷基氨基芳基衍生物
公开(公告)号：US5739158A
公开(公告)日：1998-04-14
申请号：US877190
申请日：1992-07-01
申请人： Brian R. de Costa , Kenner C. Rice , Nancy M. Gray , Patricia C. Contreras , Arthur E. Jacobson , Andrew Thurkauf , Lilian A. Radesca , Wayne D. Bowen , J. Michael Walker
发明人： Brian R. de Costa , Kenner C. Rice , Nancy M. Gray , Patricia C. Contreras , Arthur E. Jacobson , Andrew Thurkauf , Lilian A. Radesca , Wayne D. Bowen , J. Michael Walker
IPC分类号： A61K31/40 , A61K31/4025 , A61P25/00 , C07D295/12 , C07D295/135 , C07D405/12 , C07D295/073
CPC分类号： C07D295/135
摘要： Certain nitrogen-containing cyclohetero cycloalkylaminoaryl 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 ##STR1## wherein R.sup.1 is selected from hydrido, loweralkyl, cycloalkylalkyl of four to six carbon atoms and loweralkenylloweralkyl; wherein each of R.sup.2 and R.sup.3 is independently selected from hydrido and loweralkyl; wherein each of R.sup.4 through R.sup.7, R.sup.10 and R.sup.11 is independently selected from hydrido, hydroxy, loweralkyl, benzyl, phenoxy, benzyloxy and haloloweralkyl; wherein n is a number selected from four through six; wherein p is a number selected from zero through four; wherein q is a number selected from three through five; 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.
摘要翻译： PCT No.PCT / US91 / 00688 Sec。 371日期：1992年7月1日 102（e）日期1992年7月1日PCT 1991年1月31日PCT PCT。 WO91 / 12247 PCT出版物日期1991年8月22日描述了含氮环杂环烷基氨基芳基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为四氟化烷基，四至六个碳原子的环烷基烷基和低级链烯基低级烷基; 其中R2和R3各自独立地选自氢和低级烷基; 其中R 4至R 7，R 10和R 11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n是选自四至六的数字; 其中p是选自零至四的数字; 其中q是选自三至五的数; 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。

3. 发明授权

US5604255A N-(1-thienylcycloalkyl)alkenylamines for treatment of neurotoxic injury 失效
标题翻译：用于治疗神经毒性损伤的N-（1-噻吩基环烷基）烯基胺
公开(公告)号：US5604255A
公开(公告)日：1997-02-18
申请号：US344433
申请日：1994-11-23
申请人： Kenner C. Rice , Arthur E. Jacobson , Andrew Thurkauf , Mariena V. Mattson , Thomas L. O'Donohue , Patricia C. Contreras , Nancy M. Gray
发明人： Kenner C. Rice , Arthur E. Jacobson , Andrew Thurkauf , Mariena V. Mattson , Thomas L. O'Donohue , Patricia C. Contreras , Nancy M. Gray
IPC分类号： C07D333/20 , C07D409/06 , C07D409/04 , A61K31/40
CPC分类号： C07D409/06 , C07D333/20
摘要： 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 ##STR1## wherein R.sup.1 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 R.sup.2 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 R.sup.5 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
摘要翻译：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。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下式的化合物，其中R 1是一个或多个选自氢，烷基一至约五个碳原子，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; 其中R2各自为选自氢化物，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; 其中R5是一个或多个选自氢化的，一至五个碳原子的烷基，三个至五个碳原子的环烷基，二个至五个碳原子的烯基，羟基和烷氧基的基团; 并且其中所述含N环内的虚线表示任意两个相邻碳原子之间的双键

4. 发明授权

US5401755A N-(1-thienylcycloalkyl)alkenylamines for treatment of neurotoxic injury 失效
标题翻译：用于治疗神经毒性损伤的N-（1-噻吩基环烷基）烯基胺
公开(公告)号：US5401755A
公开(公告)日：1995-03-28
申请号：US774003
申请日：1991-10-08
申请人： Kenner C. Rice , Arthur E. Jacobson , Andrew Thurkauf , Mariena V. Mattson , Thomas L. O'Donohue , Patricia C. Contreras , Nancy M. Gray
发明人： Kenner C. Rice , Arthur E. Jacobson , Andrew Thurkauf , Mariena V. Mattson , Thomas L. O'Donohue , Patricia C. Contreras , Nancy M. Gray
IPC分类号： A61K31/38 , A61K31/381 , A61K31/40 , A61K31/4025 , A61K31/435 , A61K31/4433 , A61K31/445 , A61P25/00 , C07D333/20 , C07D409/06 , C07D409/08 , A61K31/44
CPC分类号： C07D409/06 , C07D333/20
摘要： 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 ##STR1## wherein R.sup.1, R.sup.2, and R.sup.5 are defined in specification.
摘要翻译：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。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（I）的化合物，其中R 1，R 2和R 5在本说明书中定义。

5. 发明授权

US5055468A Use of bridged tricyclic amine derivatives as anti-ischemic agents 失效
标题翻译：桥联三环胺衍生物作为抗缺血剂的用途
公开(公告)号：US5055468A
公开(公告)日：1991-10-08
申请号：US428531
申请日：1989-10-30
申请人： Nancy M. Gray , Patricia C. Contreras
发明人： Nancy M. Gray , Patricia C. Contreras
IPC分类号： A61K31/135 , A61K31/16 , A61K31/445 , A61K31/495 , A61K31/505
CPC分类号： A61K31/16 , A61K31/135 , A61K31/445 , A61K31/495 , A61K31/505
摘要： Certain bridged tricyclic amine compounds are described as being therapeutically effective in treatments of CNS disorders resulting from neurotoxic damage or neurodegenerative diseases, particularly those CNS disorders resulting from ischemic events. Compounds of particular interest for use as neuroprotective agents are those of the formula ##STR1## wherein each of R.sup.1 and R.sup.2 is independently selected from hydrido, loweralkyl, benzyl and phenyl; wherein each of R.sup.1 through R.sup.7 is independently selected from hydrido, loweralkyl, hydroxy, benzyl, phenyl, loweralkoxy, phenoxy, benzyloxy, halo and haloloweralkyl; wherein R.sup.18 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 X is independently one or more groups selected from hydrido, hydroxy, loweralkyl, benzyl, phenyl, loweralkoxy, phenoxy, haloloweralkyl, halo, and lower-alkanoyl; and wherein each of R.sup.23 through R.sup.30 is independently selected from hydrido, lower alkyl, benzyl, phenyl and halo; wherein R.sup.18 together with one of R.sup.23, R.sup.24, R.sup.29 or R.sup.30 may form a fused heterocyclic ring containing five or six ring members; or a pharmaceutically-acceptable salt thereof.
摘要翻译：描述了某些桥连的三环胺化合物在治疗由神经毒性损伤或神经变性疾病，特别是由缺血事件引起的CNS障碍引起的CNS障碍中的治疗有效性。用作神经保护剂的特别感兴趣的化合物是下式的化合物：其中R 1和R 2各自独立地选自氢，低级烷基，苄基和苯基; 其中R 1至R 7各自独立地选自氢，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 18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含有5-7个环成员的杂环，其中一个或两个环成员是氮原子; 其中每个X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 23至R 30各自独立地选自氢，低级烷基，苄基，苯基和卤素; 其中R 18与R 23，R 24，R 29或R 30中的一个可以形成含有五个或六个环成员的稠合杂环; 或其药学上可接受的盐。

6. 发明授权

US5192762A Use of bridged tricyclic amine derivatives as anti-ischemic agents 失效
标题翻译：桥联三环胺衍生物作为抗缺血剂的用途
公开(公告)号：US5192762A
公开(公告)日：1993-03-09
申请号：US745027
申请日：1991-08-14
申请人： Nancy M. Gray , Patricia C. Contreras
发明人： Nancy M. Gray , Patricia C. Contreras
IPC分类号： A61K31/135 , A61K31/16 , A61K31/445 , A61K31/495 , A61K31/505
CPC分类号： A61K31/495 , A61K31/135 , A61K31/16 , A61K31/445 , A61K31/505
摘要： Certain bridged tricyclic amine compounds are described as being therapeutically effective in treatment of CNS disorders resulting from neurotoxic damage or neurodegenerative diseases, particularly those CNS disorders resulting from ischemic events. Compounds of particular interest for use as neuroprotective agents are those of the formula ##STR1## wherein each of R.sup.1 and R.sup.2 is independently selected from hydrido, loweralkyl, benzyl and phenyl; wherein each of R.sup.1 through R.sup.7 is independently selected from hydrido, loweralkyl, hydroxy, benzyl, phenyl, loweralkoxy, phenoxy, benzyloxy, halo and haloloweralkyl; wherein R.sup.18 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 X is independently one or more groups selected from hydrido, hydroxy, loweralkyl, benzyl, phenyl, loweralkoxy, phenoxy, haloloweralkyl, halo, and loweralkanoyl; and wherein each of R.sup.23 through R.sup.30 is independently selected from hydrido, lower alkyl, benzyl, phenyl and halo; wherein R.sup.18 together with one of R.sup.23, R.sup.24, R.sup.29 or R.sup.30 may form a fused heterocyclic ring containing five or six ring members; or a pharmaceutically-acceptable salt thereof.
摘要翻译：描述了某些桥连三环胺化合物在治疗由神经毒性损伤或神经变性疾病，特别是由缺血事件引起的CNS障碍引起的CNS障碍中的治疗有效性。用作神经保护剂的特别感兴趣的化合物是下式的化合物：其中R 1和R 2各自独立地选自氢，低级烷基，苄基和苯基; 其中R 1至R 7各自独立地选自氢，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 18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含有5-7个环成员的杂环，其中一个或两个环成员是氮原子; 其中每个X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 23至R 30各自独立地选自氢，低级烷基，苄基，苯基和卤素; 其中R 18与R 23，R 24，R 29或R 30中的一个可以形成含有五个或六个环成员的稠合杂环; 或其药学上可接受的盐。

7. 发明授权

US5516771A Use of indolocarbazole derivatives to treat a pathological condition of the prostate 失效
标题翻译：使用吲哚并咔唑衍生物治疗前列腺的病理状况
公开(公告)号：US5516771A
公开(公告)日：1996-05-14
申请号：US250175
申请日：1994-05-27
申请人： Craig A. Dionne , Patricia C. Contreras , Chikara Murakata
发明人： Craig A. Dionne , Patricia C. Contreras , Chikara Murakata
IPC分类号： A61K31/407 , A61K31/5395 , A61K31/55 , A61K31/553 , A61P13/08 , A61P35/00 , A61P43/00 , C07D487/14 , C07D498/22 , C07H19/04
CPC分类号： C07D487/14 , A61K31/55 , C07H19/04
摘要： The invention features a method of treating a pathological condition of the prostate gland, e.g., benign prostatic hypertrophy or prostate cancer, in a mammal, said method comprising administering to said mammal a therapeutic amount of the indolocarbazole compound K-252a or a preferred derivative thereof. The invention also includes novel derivatives of K-252a.
摘要翻译：本发明的特征在于在哺乳动物中治疗前列腺的病理状况，例如良性前列腺肥大或前列腺癌的方法，所述方法包括向所述哺乳动物施用治疗量的吲哚并咔唑化合物K-252a或其优选的衍生物。本发明还包括K-252a的新型衍生物。

8. 发明授权

US5654427A Indolocarbazole derivatives to treat a pathological condition of the prostate 失效
标题翻译：吲哚咯唑衍生物治疗前列腺的病理状况
公开(公告)号：US5654427A
公开(公告)日：1997-08-05
申请号：US463680
申请日：1995-06-05
申请人： Craig A. Dionne , Patricia C. Contreras , Chikara Murakata
发明人： Craig A. Dionne , Patricia C. Contreras , Chikara Murakata
IPC分类号： A61K31/407 , A61K31/5395 , A61K31/55 , A61K31/553 , A61P13/08 , A61P35/00 , A61P43/00 , C07D487/14 , C07D498/22 , C07H19/04
CPC分类号： C07D487/14 , A61K31/55 , C07H19/04
摘要： The invention features a method of treating a pathological condition of the prostate gland, e.g., benign prostatic hypertrophy or prostate cancer, in a mammal, said method comprising administering to said mammal a therapeutic amount of the indolocarbazole compound K-252a or a preferred derivative thereof. The invention also includes novel derivatives of K-252a.
摘要翻译：本发明的特征在于在哺乳动物中治疗前列腺的病理状况，例如良性前列腺肥大或前列腺癌的方法，所述方法包括向所述哺乳动物施用治疗量的吲哚并咔唑化合物K-252a或其优选的衍生物。本发明还包括K-252a的新型衍生物。

9. 依法登记的发明

USH1899H Diagnostic uses of IGFBP-2 失效
标题翻译： IGFBP-2的诊断用途
公开(公告)号：USH1899H
公开(公告)日：2000-10-03
申请号：US827894
申请日：1996-08-22
申请人： Ratan Bhat , Matthew S. Miller , Patricia C. Contreras
发明人： Ratan Bhat , Matthew S. Miller , Patricia C. Contreras
IPC分类号： G01N33/50 , G01N33/74 , A01N37/18
CPC分类号： G01N33/74 , G01N33/5091 , G01N2333/4745
摘要： A method for determining a concentration of IGF-I that defines a therapeutically effective dose of IGF-I, i.e., a dose that will provide a therapeutic response in the treatment of neurological disorders for which IGF-I is utilized (including peripheral neuropathy, diabetic neuropathy, post-polio syndrome, small fiber neuropathy, ALS, and MS) is described. The method comprises determining whether a particular dose of IGF-I causes a 1.5 fold or greater increase in the homeostatic concentration of plasma IGFBP-2 in a mammal that has previously received a defined dose of IGF-I. The method of the invention can also be used to determine whether or not biological tolerance has developed to a particular dose of IGF-I.
摘要翻译：确定限定IGF-1的治疗有效剂量的IGF-1浓度的方法，即在治疗使用IGF-1的神经障碍（包括周围神经病，糖尿病）中提供治疗反应的剂量神经病，脊髓灰质炎综合征，小纤维神经病，ALS和MS）。该方法包括确定特定剂量的IGF-I是否先前已经接受了规定剂量的IGF-1的哺乳动物中血浆IGFBP-2的体内平衡浓度增加1.5倍或更多。本发明的方法还可以用于确定生物耐受性是否已经发展成特定剂量的IGF-1。

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