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    1-substituted-2-(N-pheny l-N-(phenylmethyl)methanamine)-4,5-dihydro-imidazoles and related compounds and their use in treating calcium overload in brain cells
    1.
    发明授权
    1-substituted-2-(N-pheny l-N-(phenylmethyl)methanamine)-4,5-dihydro-imidazoles and related compounds and their use in treating calcium overload in brain cells 失效
    1-取代-2-（N-苯基-N-（苯甲基）甲胺）-4,5-二氢咪唑及其相关化合物及其在脑细胞中治疗钙超载中的应用

    公开(公告)号：US5296493A

    公开(公告)日：1994-03-22

    申请号：US704469

    申请日：1991-05-23

    申请人： Peter Moldt ,  Elsebet O. Nielsen

    发明人： Peter Moldt ,  Elsebet O. Nielsen

    IPC分类号： C07D233/24 ,  C07D233/54 ,  C07D233/60 ,  C07D235/14 ,  C07D401/12 ,  C07D403/06 ,  C07D405/12 ,  A61K31/415 ,  A61K31/44 ,  C07D233/61 ,  C07D401/06

    CPC分类号： C07D233/64 ,  C07D233/24 ,  C07D235/14 ,  C07D401/12 ,  C07D403/06 ,  C07D405/12

    摘要： The present patent application discloses compounds of the formula ##STR1## wherein R.sup.1 is C.sub.1-10 saturated or unsaturated alkyl; or ##STR2## wherein R'" is H or ##STR3## R.sup.2 is phenyl which is unsubstituted or substituted one or more times with halogen, CF.sub.3, C.sub.1-6 -alkoxy, NO.sub.2, CO.sub.2 --C.sub.1-6 -alkyl, methyl; benzyl which may be substituted one or more times with halogen, CF.sub.3, C.sub.1-6 -alkoxy, NO.sub.2, CO.sub.2 --C.sub.1-6 -alkyl, methyl; pyridyl; or cyclohexyl;R.sup.3 phenyl which is unsubstituted or substituted one or more times with halogen, CF.sub.3, C.sub.1-6 -alkoxy, NO.sub.2, CO.sub.2 --C.sub.1-6 -alkyl, methyl; naphthyl which may be substituted one or more times with halogen, CF.sub.3, C.sub.1-6 -alkoxy, NO.sub.2, CO.sub.2 --C.sub.1-6 -alkyl, methyl; pyridyl; C.sub.1-6 unsaturated alkyl; furanyl;R.sup.4 is H, C.sub.1-6 -alkyl, or benzyl; or ##STR4## together form ##STR5## R' and R" are each hydrogen or together form an extra benzo ring; and wherein the dotted line represents an optional extra bond between the two carbon atoms designated .alpha. and .beta.,or a pharmaceutically-acceptable addition salt thereof.The compounds are useful as pharmaceuticals, for example in the treatment of Ca overload in brain cells.

    摘要翻译： 本专利申请公开了式IMA的化合物，其中R 1是C 1-10饱和或不饱和的烷基; 或者其中R“'为H或R 2是未被取代或被卤素，CF 3，C 1-6 - 烷氧基，NO 2，CO 2 -C 1-6 - 烷基，甲基取代或被取代的苯基。 可以被卤素，CF 3，C 1-6 - 烷氧基，NO 2，CO 2 -C 1-6 - 烷基，甲基取代一次或多次的苄基; 吡啶基 或环己基; R 3苯基，其未被取代或被卤素，CF 3，C 1-6 - 烷氧基，NO 2，CO 2 -C 1-6烷基，甲基取代一次或多次; 可以被卤素，CF 3，C 1-6 - 烷氧基，NO 2，CO 2 -C 1-6 - 烷基，甲基取代一次或多次的萘基; 吡啶基 C 1-6不饱和烷基; 呋喃基 R4是H，C1-6烷基或苄基; 或一起形成 R'和R“各自为氢或一起形成额外的苯并环; 并且其中虚线表示指定为α和β的两个碳原子之间的任选的额外键或其药学上可接受的加成盐。 这些化合物可用作药物，例如用于治疗脑细胞中的Ca超载。

    HYDROCHLORIDE SALT OF AN AZABICYCLO[3.2.1]OCTANE DERIVATIVE
    2.
    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。

    Non-injection immunotherapy
    3.
    发明申请
    Non-injection immunotherapy 审中-公开
    非注射免疫治疗

    公开(公告)号：US20060269576A1

    公开(公告)日：2006-11-30

    申请号：US11140457

    申请日：2005-05-27

    申请人： Peter Moldt ,  Ove Pedersen ,  Klaus Theobald ,  Michael Flanagan

    发明人： Peter Moldt ,  Ove Pedersen ,  Klaus Theobald ,  Michael Flanagan

    IPC分类号： A61K39/35 ,  A61K39/36

    CPC分类号： A61K39/35 ,  A61K39/36 ,  A61K2039/54

    摘要： Methods and compositions are disclosed for the reduction of immune responses to an exogenous allergen. The reduction is obtained by pre-treatment or pre-conditioning, without injection, of a subject with the allergen so as to reduce immune responses in the subject upon additional exposure to the allergen. The invention is advantageously used in a variety of contexts, including seasonal allergies wherein pre-treatment or pre-conditioning is performed before the onset of the seasonal allergy.

    摘要翻译： 公开了减少对外源性变应原的免疫应答的方法和组合物。 通过预处理或预处理而不注射受试者与变应原来获得还原，以便在额外暴露于变应原时降低受试者的免疫应答。 本发明有利地用于各种情况，包括在季节性变态反应发作之前进行预处理或预处理的季节性过敏。

    Fused indole and quinoxaline derivatives, their preparation and use
    4.
    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。

    Tropane-derivatives, their preparation and use
    6.
    发明授权
    Tropane-derivatives, their preparation and use 失效
    托烷衍生物，其制备和用途

    公开(公告)号：US06395748B2

    公开(公告)日：2002-05-28

    申请号：US09814413

    申请日：2001-03-21

    申请人： Jørgen Scheel-Krüger ,  Peter Moldt ,  Frank Wätjen

    发明人： Jørgen Scheel-Krüger ,  Peter Moldt ,  Frank Wätjen

    IPC分类号： A61K3146

    CPC分类号： C07D451/02 ,  C07D451/00

    摘要： Compounds of formula (a), (b), (c), or (d), or any mixture thereof, or a pharmaceutically-acceptable salt thereof; wherein R is hydrogen, alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkylalkyl or 2-hydroxyethyl; R3 is —CH2—X—R′, wherein X is O, S or NR″, wherein R″ is hydrogen or alkyl and R′ is alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkylalkyl, or —CO-alkyl; R4 is phenyl optionally substituted with halogen, CF3, CN, alkoxy, cycloalkoxy, alkyl, cycloalkyl, alkenyl, alkynyl, amino, nitro, heteroaryl, or aryl; 3,4-methylenedioxyphenyl; benzyl optionally substituted with halogen, CF3, CH, alkoxy, cycloalkoxy, alkyl, cycloalkyl, alkenyl, alkynyl, amino, nitro, heteroaryl, or aryl; heteroaryl optionally substituted with halogen, CF3, CN, alkoxy, cycloalkoxy, alkyl, cycloalkyl, alkenyl, alkynyl, amino, nitro, heteroaryl, or aryl; or naphthyl optionally substituted with halogen, CF3, CN, alkoxy, cycloalkoxy, alkyl, cycloalkyl, alkenyl, alkynyl, amino, nitro, heteroaryl, or aryl. The compounds are monoamine neurotransmitter, i.e., dopamine, serotonin, noradrenaline, reuptake inhibitors.

    摘要翻译： 式（a），（b），（c）或（d）的化合物或其任何混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-CH2-X-R'，其中X是O，S或NR“，其中R”是氢或烷基，R'是烷基，烯基，炔基，环烷基，环烷基烷基或-CO-烷基; R4是任选被卤素，CF 3，CN，烷氧基，环烷氧基，烷基，环烷基，烯基，炔基，氨基，硝基，杂芳基或芳基取代的苯基; 3,4-亚甲二氧基苯基; 任选被卤素，CF 3，CH，烷氧基，环烷氧基，烷基，环烷基，烯基，炔基，氨基，硝基，杂芳基或芳基取代的苄基; 任选被卤素，CF 3，CN，烷氧基，环烷氧基，烷基，环烷基，烯基，炔基，氨基，硝基，杂芳基或芳基取代的杂芳基; 或任选被卤素，CF 3，CN，烷氧基，环烷氧基，烷基，环烷基，烯基，炔基，氨基，硝基，杂芳基或芳基取代的萘基。 化合物是单胺神经递质，即多巴胺，5-羟色胺，去甲肾上腺素，再摄取抑制剂。

    Piperidine derivatives as neurotransmitter re-uptake inhibitors
    7.
    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。

    Method for the preparation of esters of anhydroecgonine
    8.
    发明授权
    Method for the preparation of esters of anhydroecgonine 失效
    制备脱氢gon of酯的方法

    公开(公告)号：US5990312A

    公开(公告)日：1999-11-23

    申请号：US913446

    申请日：1997-11-04

    申请人： Peter Moldt

    发明人： Peter Moldt

    IPC分类号： C07D451/02 ,  C07D451/10

    CPC分类号： C07D451/02

    摘要： The present invention discloses compounds of the formula any mixture thereof, or a pharmaceutically acceptable salt thereof;wherein R, R.sup.3, and R.sup.4 each have the meanings set forth in the specification.The compounds possess valuable pharmaceutical properties as dopamine reuptake inhibitors.

    摘要翻译： PCT No.PCT / EP96 / 01277 Sec。 371日期1997年11月4日 102（e）日期1997年11月4日PCT PCT 1996年3月22日PCT公布。 WO96 / 30371 PCT出版物 日期：1996年10月3日本发明公开了下式的化合物或其药学上可接受的盐： 其中R，R 3和R 4各自具有说明书中阐述的含义。 该化合物具有有价值的药物性质作为多巴胺再摄取抑制剂。