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    HYDROCHLORIDE SALT OF AN AZABICYCLO[3.2.1]OCTANE DERIVATIVE
    1.
    发明申请
    HYDROCHLORIDE SALT OF AN AZABICYCLO[3.2.1]OCTANE DERIVATIVE 有权
    亚硫酸氢盐的盐酸盐[3.2.1]月桂衍生物

    公开(公告)号：US20100056561A1

    公开(公告)日：2010-03-04

    申请号：US12529502

    申请日：2008-02-28

    申请人： Trevor John Grinter ,  Peter Moldt ,  Frank Watjen

    发明人： Trevor John Grinter ,  Peter Moldt ,  Frank Watjen

    IPC分类号： A61K31/46 ,  C07D451/02 ,  A61P25/00

    CPC分类号： C07D451/02

    摘要： The invention relates to a hydrochloride salt of (1R,2R,3S,5S)-3-(3,4-dichlorophenyl)-2-[(methyloxy)methyl]-8-azabicyclo[3.2.1]octane, uses of the salt as a medicament in the treatment inter alia of disorders of the central nervous system and pharmaceutical compositions and dosage forms comprising the salt.

    摘要翻译： 本发明涉及（1R，2R，3S，5S）-3-（3,4-二氯苯基）-2 - [（甲氧基）甲基] -8-氮杂双环[3.2.1]辛烷的盐酸盐， 盐作为治疗特别是中枢神经系统病症的药物以及包含该盐的药物组合物和剂型。

    Hydrochloride salt of an azabicyclo[3.2.1]octane derivative
    2.
    发明授权
    Hydrochloride salt of an azabicyclo[3.2.1]octane derivative 有权
    氮杂双环[3.2.1]辛烷衍生物的盐酸盐

    公开(公告)号：US08263611B2

    公开(公告)日：2012-09-11

    申请号：US12529502

    申请日：2008-02-28

    申请人： Trevor John Grinter ,  Peter Moldt ,  Frank Watjen

    发明人： Trevor John Grinter ,  Peter Moldt ,  Frank Watjen

    IPC分类号： A61K31/46 ,  C07D451/02 ,  A61P25/00

    CPC分类号： C07D451/02

    摘要： The invention relates to a hydrochloride salt of (1R,2R,3S,5S)-3-(3,4-dichlorophenyl)-2-[(methyloxy)methyl]-8-azabicyclo[3.2.1]octane, uses of the salt as a medicament in the treatment inter alia of disorders of the central nervous system and pharmaceutical compositions and dosage forms comprising the salt.

    摘要翻译： 本发明涉及（1R，2R，3S，5S）-3-（3,4-二氯苯基）-2 - [（甲氧基）甲基] -8-氮杂双环[3.2.1]辛烷的盐酸盐， 盐作为治疗特别是中枢神经系统病症的药物以及包含该盐的药物组合物和剂型。

    Piperidine derivatives as neurotransmitter re-uptake inhibitors
    4.
    发明授权
    Piperidine derivatives as neurotransmitter re-uptake inhibitors 失效
    哌啶衍生物作为神经递质再摄取抑制剂

    公开(公告)号：US06376673B1

    公开(公告)日：2002-04-23

    申请号：US09415227

    申请日：1999-10-12

    申请人： Peter Moldt ,  Frank Watjen ,  Jorgen Scheel-Kruger

    发明人： Peter Moldt ,  Frank Watjen ,  Jorgen Scheel-Kruger

    IPC分类号： C07D21118

    CPC分类号： C07D211/28

    摘要： The present invention relates to compounds of formula (I), or a pharmaceutically acceptable salt thereof; wherein R is hydrogen, alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkylalkyl or 2-hydroxyethyl; R3 is —CR′═NOR″ wherein R′ and R″ each independently are hydrogen, alkyl, cycloalkyl, cycloalkylalkyl, alkenyl, cycloalkylalkenyl, alkynyl, cycloalkylalkynyl, aryl or benzyl; R4 is phenyl which may be substituted one or more times with substituents selected from the group consisting of halogen, CF3, CN, amino, nitro, alkoxy, cycloalkoxy, alkyl, cycloalkyl, alkenyl, alkynyl, aryl and heteroaryl; 3,4-methylenedioxyphenyl; benzyl which may be substituted one or more times with substituents selected from the group consisting of halogen, CF3, CN, amino, nitro, alkoxy, cycloalkoxy, alkyl, cycloalkyl, alkenyl, alkynyl, aryl and heteroaryl; heteroaryl which may be substituted one or more times with substituents selected from the group consisting of halogen, CF3, CN, amino, nitro, alkoxy, cycloalkoxy, alkyl, cycloalkyl, alkenyl, alkynyl, aryl and heteroaryl; or naphthyl which may be substituted one or more times with substituents selected from the group consisting of halogen, CF3, CN, amino, nitro, alkoxy, cycloalkoxy, alkyl, cycloalkyl, alkenyl, alkynyl, aryl and heteroaryl. The compounds possess valuable pharmaceutical properties as monoamine neurotransmitter, i.e. dopamine, serotonin, noradrenaline, reuptake inhibitors.

    摘要翻译： 本发明涉及式（I）化合物或其药学上可接受的盐; 其中R是氢，烷基，烯基，炔基，环烷基，环烷基烷基或2-羟乙基; R3是-CR'= NOR“，其中R'和R”各自独立地为氢，烷基，环烷基，环烷基烷基，烯基，环烷基烯基，炔基，环烷基炔基，芳基或苄基; R4是可以被选自卤素，CF 3，CN，氨基，硝基，烷氧基，环烷氧基，烷基，环烷基，烯基，炔基，芳基和杂芳基的取代基取代一次或多次的苯基; 3,4-亚甲二氧基苯基; 苄基，其可以被选自卤素，CF 3，CN，氨基，硝基，烷氧基，环烷氧基，烷基，环烷基，烯基，炔基，芳基和杂芳基的取代基取代一次或多次; 可以被选自卤素，CF 3，CN，氨基，硝基，烷氧基，环烷氧基，烷基，环烷基，烯基，炔基，芳基和杂芳基的取代基取代一次或多次的杂芳基; 或萘基，其可以被选自卤素，CF 3，CN，氨基，硝基，烷氧基，环烷氧基，烷基，环烷基，烯基，炔基，芳基和杂芳基的取代基取代一次或多次。 该化合物具有作为单胺神经递质（即多巴胺，5-羟色胺，去甲肾上腺素，再摄取抑制剂）的有价值的药物性质。

    Fused indole and quinoxaline derivatives, their preparation and use
    5.
    发明授权
    Fused indole and quinoxaline derivatives, their preparation and use 失效
    熔融吲哚和喹喔啉衍生物，其制备和使用

    公开(公告)号：US5801174A

    公开(公告)日：1998-09-01

    申请号：US809086

    申请日：1997-05-20

    申请人： Peter Moldt ,  Frank Watjen

    发明人： Peter Moldt ,  Frank Watjen

    IPC分类号： A61K31/40 ,  A61K31/407 ,  A61K31/435 ,  A61K31/437 ,  A61K31/55 ,  A61P9/00 ,  A61P9/08 ,  A61P9/10 ,  A61P25/00 ,  A61P25/04 ,  A61P25/08 ,  A61P25/16 ,  A61P25/18 ,  A61P25/20 ,  A61P25/22 ,  A61P25/28 ,  A61P25/30 ,  A61P39/02 ,  C07D471/04 ,  C07D487/04 ,  A61K31/495

    CPC分类号： C07D471/04 ,  C07D487/04

    摘要： The present patent application discloses compounds having the formula ##STR1## or a pharmaceutically acceptable salt thereof wherein R.sup.1 is hydrogen, alkyl or benzyl; X is O or NOR.sup.2, wherein R.sup.2 is hydrogen, alkyl or benzyl; Y is N--R.sup.4 wherein R.sup.4 is hydrogen, OH or alkyl; n is 0 or 1; R.sup.6 is phenyl which is substituted one or more times with substituents selected from the group consisting of SO.sub.2 NR'R", CONR'R", and COR'" wherein R' and R" each independently are hydrogen, alkyl, or --(CH.sub.2).sub.p --W, wherein p is 0, 1, 2, 3, 4, 5, or 6, and W is hydroxy, amino, alkoxycarbonyl, or phenyl which may be substituted one or more times with substituents selected from the group consisting of halogen, CF.sub.3, NO.sub.2, amino, alkyl, alkoxy or methylenedioxy; or wherein R' and R" together is (CH.sub.2).sub.r Z(CH.sub.2).sub.s wherein r and s each independently are 0, 1, 2, 3, 4, 5, or 6 and Z is O, S, CH.sub.2 or NR"" wherein R"" is hydrogen, alkyl, or --(CH.sub.2).sub.p --W, wherein p is 0, 1, 2, 3, 4, 5, or 6, and W is hydroxy, amino, alkoxycarbonyl, or phenyl which may be substituted one or more times with substituents selected from the group consisting of halogen, CF.sub.3, NO.sub.2, amino, alkyl, alkoxy or methylenedioxy; and wherein R'" is hydrogen, alkyl, alkoxy or phenyl which may be substituted one or more times with substituents selected from the group consisting of halogen, CF.sub.3, NO.sub.2, amino, alkyl, alkoxy or methylenedioxy; A is a ring of five to seven atoms fused with the benzo ring at the positions marked a and b. The compounds are useful in the treatment of cerebrovascular disorders for example.

    摘要翻译： PCT No.PCT / EP95 / 03594 371日期1997年5月20日 102（e）日期1997年5月20日PCT提交1995年9月12日PCT公布。 出版物WO96 / 08495 日本特开1996年3月21日本专利申请公开了具有式“IMAGE”的化合物或其药学上可接受的盐，其中R 1是氢，烷基或苄基; X是O或NOR2，其中R2是氢，烷基或苄基; Y是N-R4，其中R4是氢，OH或烷基; n为0或1; R6是被选自SO2NR'R“，CONR'R”和COR“的取代基一次或多次的苯基，其中R'和R”各自独立地是氢，烷基或 - （CH 2）p W，其中p是0,1,2,3,4,5或6，并且W是羟基，氨基，烷氧基羰基或苯基，其可以被选自以下的取代基取代一次或多次： 的卤素，CF 3，NO 2，氨基，烷基，烷氧基或亚甲二氧基; 或其中R'和R“一起是（CH 2）rZ（CH 2）s，其中r和s各自独立地是0,1,2,3,4,5或6，Z是O，S，CH 2或NR' “其中R”“是氢，烷基或 - （CH 2）p W，其中p是0,1,2,3,4,5或6，并且W是羟基，氨基，烷氧基羰基或苯基 其可以被选自卤素，CF 3，NO 2，氨基，烷基，烷氧基或亚甲二氧基的取代基取代一次或多次; 并且其中R“是氢，烷基，烷氧基或苯基，其可以被选自卤素，CF 3，NO 2，氨基，烷基，烷氧基或亚甲二氧基的取代基取代一次或多次; A是在标记a和b的位置与苯环稠合的5至7个原子的环。 该化合物可用于治疗例如脑血管障碍。

    Benzimidazole derivatives and pharmaceutical compositions comprising these compounds
    7.
    发明授权
    Benzimidazole derivatives and pharmaceutical compositions comprising these compounds 失效
    苯并咪唑衍生物和包含这些化合物的药物组合物

    公开(公告)号：US06649609B2

    公开(公告)日：2003-11-18

    申请号：US10012490

    申请日：2001-12-12

    申请人： Lene Teuber ,  Frank Watjen

    发明人： Lene Teuber ,  Frank Watjen

    IPC分类号： C07D23506

    CPC分类号： C07D235/06 ,  C07D231/12 ,  C07D233/56 ,  C07D249/08 ,  C07D401/10 ,  C07D401/12 ,  C07D403/10 ,  C07D403/12 ,  C07D405/04 ,  C07D405/12 ,  C07D405/14 ,  C07D409/12 ,  C07D413/12 ,  C07D413/14

    摘要： The present invention relates to novel 1-phenylbenzimidazole derivatives having particular alkoxycarbonyl substituents in the 5-position of the benz ring and having particular cyclic substituents in the meta-position of the phenyl ring, as well as to pharmaceutical compositions containing these compounds and to methods of treatment therewith. The compounds of the invention are useful in the treatment of central nervous system diseases and disorders, which are responsive to modulation of GABAA receptor complex, and in particular for inducing and maintaining anaesthesia, sedation, and muscle relaxation, as well as for combating febrile convulsions in children. The compounds of the invention may also be used by veterinarians.

    摘要翻译： 本发明涉及在苯环的5-位上具有特定的烷氧基羰基取代基并且在苯环的间位具有特定的环状取代基的新的1-苯基苯并咪唑衍生物以及含有这些化合物的药物组合物和方法 的治疗。 本发明的化合物可用于治疗中枢神经系统疾病和病症，其对GABAα受体复合物的调节有反应，特别是诱导和维持麻醉，镇静和肌肉松弛以及对于 打击儿童发热性惊厥。 本发明的化合物也可以由兽医使用。

    AMPA antagonists and a method of treatment
    8.
    发明授权
    AMPA antagonists and a method of treatment 失效
    AMPA拮抗剂和治疗方法

    公开(公告)号：US5843945A

    公开(公告)日：1998-12-01

    申请号：US951059

    申请日：1997-10-15

    申请人： Frank Watjen ,  Jorgen Drejer

    发明人： Frank Watjen ,  Jorgen Drejer

    IPC分类号： C07D471/04 ,  C07D487/04 ,  A61K31/55 ,  A61K31/495 ,  C07D487/00

    CPC分类号： C07D471/04 ,  C07D487/04

    摘要： The present patent application discloses compounds having formula (I) or a pharmaceutically acceptable salt thereof wherein R.sup.1 is hydrogen, alkyl or benzyl; X is O or NOR.sup.2, wherein R.sup.2 is hydrogen, alkyl or benzyl; Y is N--R.sup.4 wherein R.sup.4 is hydrogen, OH or alkyl; n is 0 or 1; R.sup.6 is phenyl, naphthyl, thienyl, pyridyl, all of which may be substituted one or more times with substituents selected from the group consisting of halogen, CF.sub.3, NO.sub.2, amino, alkyl, alkoxy and phenyl; A is a ring of five to seven atoms fused with the benzo ring at the positions marked a and b. The compounds are useful in the treatment of cerebrovascular disorders. ##STR1##

    摘要翻译： 本专利申请公开了具有式（I）的化合物或其药学上可接受的盐，其中R 1是氢，烷基或苄基; X是O或NOR2，其中R2是氢，烷基或苄基; Y是N-R4，其中R4是氢，OH或烷基; n为0或1; R6是苯基，萘基，噻吩基，吡啶基，它们都可以被选自卤素，CF 3，NO 2，氨基，烷基，烷氧基和苯基的取代基取代一次或多次; A是在标记a和b的位置与苯环稠合的5至7个原子的环。 该化合物可用于治疗脑血管障碍。

    AMPA antagonists and method of treatment therewith
    9.
    发明授权
    AMPA antagonists and method of treatment therewith 失效
    AMPA拮抗剂及其治疗方法

    公开(公告)号：US5780493A

    公开(公告)日：1998-07-14

    申请号：US951821

    申请日：1997-10-16

    申请人： Frank Watjen ,  Jorgen Drejer

    发明人： Frank Watjen ,  Jorgen Drejer

    IPC分类号： C07D471/04 ,  C07D487/04 ,  A61K31/40 ,  A61K31/44 ,  C07D401/00 ,  C07D487/02

    CPC分类号： C07D471/04 ,  C07D487/04

    摘要： The present patent application discloses compounds having formula (I) or a pharmaceutically acceptable salt thereof wherein R.sup.1 is hydrogen, alkyl or benzyl; X is O or NOR.sup.2, wherein R.sup.2 is hydrogen, alkyl or benzyl; Y is N--R.sup.4 wherein R.sup.4 is hydrogen, OH or alkyl; n is 0 or 1; R.sup.6 is phenyl, naphthyl, thienyl, pyridyl, all of which may be substituted one or more times with substituents selected from the group consisting of halogen; CF.sub.3, NO.sub.2, amino, alkyl, alkoxy and phenyl; A is a ring of five to seven atoms fused with the benzo ring at the positions marked a and b. The compounds are useful in the treatment of cerebrovascular disorders for example. ##STR1##

    摘要翻译： 本专利申请公开了具有式（I）的化合物或其药学上可接受的盐，其中R 1是氢，烷基或苄基; X是O或NOR2，其中R2是氢，烷基或苄基; Y是N-R4，其中R4是氢，OH或烷基; n为0或1; R6是苯基，萘基，噻吩基，吡啶基，它们都可以被选自卤素的取代基取代一次或多次; CF 3，NO 2，氨基，烷基，烷氧基和苯基; A是在标记a和b的位置与苯环稠合的5至7个原子的环。 该化合物可用于治疗例如脑血管障碍。 （一）

    Isatinoxime derivatives, their preparation and use
    10.
    发明授权
    Isatinoxime derivatives, their preparation and use 失效
    伊马替尼衍生物，其制备和用途

    公开(公告)号：US5242918A

    公开(公告)日：1993-09-07

    申请号：US936579

    申请日：1992-08-27

    申请人： Frank Watjen ,  Bjarne H. Dahl ,  Jorgen Drejer ,  Leif H. Jensen

    发明人： Frank Watjen ,  Bjarne H. Dahl ,  Jorgen Drejer ,  Leif H. Jensen

    IPC分类号： C07C205/45 ,  C07D471/04 ,  C07D487/04 ,  C07D491/04 ,  C07D491/048 ,  C07D495/04

    CPC分类号： C07D471/04 ,  C07C205/45 ,  C07D487/04 ,  C07D491/04 ,  C07D495/04

    摘要： A compound having the formula ##STR1## wherein R.sup.4 and R.sup.5 independently are hydrogen, halogen, CF.sub.3, CN, NO.sub.2 or SO.sub.2 NR.sup.1 R.sup.2 whereinR.sup.1 is hydrogen or straight, C.sub.1-6 -alkyl which may be branched or cyclic,R.sup.2 is hydrogen or straight, C.sub.1-6 -alkyl which may be branched or cyclic,or wherein R.sup.1 and R.sup.2 together represent --(CH.sub.2).sub.n --A--(CH.sub.2).sub.m --, wherein A is O, S, CH.sub.2 or NR.sup.I, wherein R.sup.I is H, C.sub.1-6 -alkyl which may be straight, branched or cyclic, n is 0, 1, 2, 3, 4, 5 and m is 0, 1, 2, 3, 4, 5;Q is NOH or O;Z=O, S, N--R.sup.II, ##STR2## wherein R.sup.II, R.sup.III, R.sup.IV and R.sup.V independently are hydrogen, benzyl, C.sub.1-6 carboxylic acid-acyl, C.sub.1-6 -alkoxy which may be branched or cyclic, or C.sub.1-6 -alkyl which may be branched or cyclic;X is --(CH.sub.2).sub.o -- wherein o is 0, 1, 2, or 3;Y is --(CH.sub.2).sub.p -- wherein p is 0, 1, 2 or 3;.alpha. and .beta. indicate attachment points,and a method of treating disorders of a mammal, including a human, responsive to the blockade of glutamic and aspartic acid receptors, with the same.

    摘要翻译： 具有式“IMAGE”的化合物，其中R 4和R 5独立地是氢，卤素，CF 3，CN，NO 2或SO 2 NR 1 R 2，其中R 1是氢或直链，可以是支链或环状的C 1-6 - 烷基，R 2是氢或直链， 可以是支链或环状的C 1-6 - 烷基，或其中R 1和R 2一起表示 - （CH 2）nA-（CH 2）m - ，其中A是O，S，CH 2或NRI，其中R 1是H，C 1-6 - 烷基，其可以是直链，支链或环状的，n为0,1,2,3,4,5，m为0,1,2,3,4,5; Q是NOH或O; Z = O，S，N-RII，其中RII，RIII，RIV和RV独立地是氢，苄基，C1-6羧酸 - 酰基，可以是支链或环状的C1-6 - 烷氧基或C1-6 可以是支链或环状的 - 烷基; X是 - （CH 2）o - ，其中o是0,1,2或3; Y是 - （CH 2）p - ，其中p是0,1,2或3; α和β表示连接点，以及一种治疗对谷氨酸和天冬氨酸受体的封闭有反应的哺乳动物（包括人）的病症的方法。