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11 条记录 (耗时 0.017 秒)

    Novel intermediate and method for its preparation
    2.
    发明授权
    Novel intermediate and method for its preparation 失效
    新型中间体及其制备方法

    公开(公告)号：US4650884A

    公开(公告)日：1987-03-17

    申请号：US761774

    申请日：1985-08-02

    申请人： Klaus P. Bogeso

    发明人： Klaus P. Bogeso

    IPC分类号： A61K31/34 ,  A61K31/343 ,  A61P25/24 ,  A61P25/26 ,  C07C67/00 ,  C07C253/00 ,  C07C253/30 ,  C07C255/51 ,  C07C255/59 ,  C07D307/87 ,  C07F3/02 ,  C07C121/80

    CPC分类号： C07D307/87 ,  C07C255/00

    摘要： The present invention relates to the novel compound of the following formula: ##STR1## as well as acid addition salts thereof, a method for the preparation of the compound of Formula I, and to the use of said novel compound in the preparation of the known antidepressant drug 1-(3-dimethylaminopropyl)-1-(4'-fluorophenyl)-1,3-dihydroisobenzofuran-5-carbonitrile, or a pharmaceutically acceptable acid addition salt thereof.

    摘要翻译： 本发明涉及下式的新型化合物：其中R 1，R 2，及其酸加成盐，式Ⅰ化合物的制备方法，以及所述新型化合物在制备式 已知的抗抑郁药物1-（3-二甲基氨基丙基）-1-（4'-氟苯基）-1,3-二氢异苯并呋喃-5-甲腈或其药学上可接受的酸加成盐。

    2-Methylthio-6-fluoro-9-(1-methyl-4-piperidylidene)-thioxanthene and salts thereof, neuroleptic compositions and method of use
    3.
    发明授权
    2-Methylthio-6-fluoro-9-(1-methyl-4-piperidylidene)-thioxanthene and salts thereof, neuroleptic compositions and method of use 失效
    2-甲硫基-6-氟-9-（1-甲基-4-哌啶基） - 噻吨酮及其盐，神经安定剂组合物和使用方法

    公开(公告)号：US4235916A

    公开(公告)日：1980-11-25

    申请号：US971509

    申请日：1978-12-20

    申请人： Klaus P. Bogeso

    发明人： Klaus P. Bogeso

    IPC分类号： A61K31/4433 ,  A61K31/445 ,  A61P25/00 ,  C07D409/04 ,  A61K31/38 ,  C07D417/04

    CPC分类号： C07D409/04

    摘要： The present invention relates to the novel compound 2-methylthio-6-fluoro-9-(1-methyl-4-piperidylidene)-thioxanthene of the formula ##STR1## and its non-toxic acid addition salts, which compounds have strong and longlasting neuroleptic properties and, at the same time, a low degree of undesired side effects such as extrapyrimidal side effects.The invention moreover relates to a method for the preparation of said novel compounds, pharmaceutical compositions containing same, which may be administered to animals, including human beings, orally or parentally.Further the invention relates to a method for producing an antipsychotic effect in warmblooded animals by administering to said animals an antipsychotically effective amount of one of said novel compounds.

    摘要翻译： 本发明涉及式I的新化合物2-甲硫基-6-氟-9-（1-甲基-4-哌啶基） - 噻吨酮及其无毒酸加成盐，该化合物具有较强的和 长期的精神安定药物性质，并且同时具有低度不期望的副作用，例如外消旋副作用。 本发明还涉及制备所述新型化合物的方法，含有该化合物的药物组合物，其可以口服或亲本施用于动物，包括人类。 此外，本发明涉及通过对所述动物施用抗精神病药有效量的所述新化合物之一来在温血动物中产生抗精神病作用的方法。

    Aminoalkyl substituted urea derivatives and method of treatment
    4.
    发明授权
    Aminoalkyl substituted urea derivatives and method of treatment 失效
    氨基烷基取代的脲衍生物和处理方法

    公开(公告)号：US4650900A

    公开(公告)日：1987-03-17

    申请号：US814664

    申请日：1985-12-30

    申请人： Niels Lassen ,  Klaus P. Bogeso ,  Klaus G. Jensen

    发明人： Niels Lassen ,  Klaus P. Bogeso ,  Klaus G. Jensen

    IPC分类号： A61K31/17 ,  A61K31/445 ,  A61P35/00 ,  C07C275/24 ,  C07D295/12 ,  C07D295/13 ,  C07C127/17 ,  C07D239/02

    CPC分类号： C07D295/13 ,  C07C275/24

    摘要： The present invention relates to novel amino alkyl substituted urea derivatives as well as their acid addition salts with pharmaceutically acceptable acids, to methods for the preparation of said derivatives and pharmaceutical compositions containing same, and a method for the treatment of tumors therewith.The novel urea derivatives have shown pronounced anti-neoplastic activity when tested against various tumor models in animals.The novel compounds of the present invention may be represented by the following formula: ##STR1## wherein X and Y are the same or different and are selected from the group consisting of a phenyl group, each of said phenyl groups being optionally substituted with one or two groups selected from halogen, CF.sub.3, OH, or alkoxy (1-4 C-atoms); and R.sup.1 and R.sup.2 are the same or different, and are each selected from the group consisting of lower alkyl groups having from one to four carbon atoms inclusive, or they form together with the nitrogen atom a saturated five- or six-membered heterocyclic ring; R.sup.3 and R.sup.4 are each selected from hydrogen, lower alkyl or alkenyl groups with from 1-6 carbon atoms inclusive, cyclopentyl or cyclohexyl; and n is 0 or 1, as well as pharmaceutically acceptable acid addition salts thereof.When X is different from Y and/or R.sup.3 is different from R.sup.4 the compounds of Formula I exist as optical isomers, which may be separated in the individual enantiomers, which often show the activity in different degree. These individual isomers as well as their isolation fall within the scope of the present invention.

    摘要翻译： 本发明涉及新的氨基烷基取代的脲衍生物及其与药学上可接受的酸的酸加成盐，所述衍生物的制备方法和含有该衍生物的药物组合物，以及用于治疗肿瘤的方法。 当针对动物中的各种肿瘤模型进行测试时，新型尿素衍生物显示明显的抗肿瘤活性。 本发明的新化合物可以由下式表示：其中X和Y相同或不同，并且选自苯基，所述苯基中的每一个任选被一个取代基 或选自卤素，CF 3，OH或烷氧基（1-4个C原子）的两个基团; 并且R 1和R 2相同或不同，并且各自选自具有1至4个碳原子的低级烷基，或者它们与氮原子一起形成饱和的五元或六元杂环; R3和R4各自选自氢，具有1-6个碳原子的低级烷基或烯基，环戊基或环己基; 和n为0或1，以及其药学上可接受的酸加成盐。 当X与Y不同且/或R 3不同于R 4时，式I化合物作为光学异构体存在，其可以在单独的对映异构体中分离，其通常以不同程度显示活性。 这些单个异构体以及它们的分离属于本发明的范围。

    Xanthene and thioxanthene derivatives
    5.
    发明授权
    Xanthene and thioxanthene derivatives 失效
    呫吨和噻吨衍生物

    公开(公告)号：US4275209A

    公开(公告)日：1981-06-23

    申请号：US106353

    申请日：1979-12-21

    申请人： Niels Lassen ,  Klaus P. Bogeso ,  Peter B. Hansen ,  Jorn L. M. Buus ,  Allan J. Bigler

    发明人： Niels Lassen ,  Klaus P. Bogeso ,  Peter B. Hansen ,  Jorn L. M. Buus ,  Allan J. Bigler

    IPC分类号： C07D409/04 ,  A01N43/40 ,  A61K31/435 ,  A61P25/18 ,  C07D335/16 ,  C07D335/18 ,  C07D405/04 ,  C07D409/06 ,  C07D409/14 ,  C07D413/14 ,  C07D417/04

    CPC分类号： C07D335/18 ,  C07C309/00 ,  C07C323/00

    摘要： The present invention relates to novel thioxanthene and xanthene derivatives which have useful pharmacodynamic activity, such as neuroleptic activity and antiemetic activity, methods for the preparation of said derivatives, pharmaceutical compositions containing same, and a method for the treatment of psychic disorders by administering a therapeutically active amount of one of said derivatives to a living animal body, including human beings.The new compounds of the present invention corresponds to the Formula I: ##STR1## wherein X is a halogen atom, an alkyl group with from one to four carbon atoms inclusive, an alkyloxy group with from one to four carbon atoms inclusive, a methylthio group, a methylsulphonyl group, a dimethylsulfamoyl group, a trifluoromethyl group or an acetyl group;Y is hydrogen, fluorine or a methyl group;Z is oxygen or sulphur;n is an integer from zero to three inclusive, andR is a cycloalkyl group with from four to six carbon atoms inclusive in the ring substituted with from one to four substituents selected from optionally esterified hydroxy- or hydroxymethyl groups, methyl groups, amino groups, acetamido groups, mesylamino groups or oxo groups, a five- or six-membered saturated heterocyclic ring having one or two heteroatoms selected from oxygen and nitrogen atoms and being optionally substituted with an optionally esterified hydroxy group or oxo group, any esterified hydroxy group present being an ester of an aliphatic carboxylic acid having from ten to twentytwo carbon atoms inclusive, as well as their non-toxic pharmaceutically acceptable acid addition salts.

    摘要翻译： 本发明涉及具有有用的药效学活性的新型噻吨酮和呫吨衍生物，例如精神安定药活性和止吐活性，制备所述衍生物的方法，含有该衍生物的药物组合物，以及通过施用治疗性的方法治疗精神疾病的方法 将一种所述衍生物的活性量提供给包括人在内的活体动物体。 本发明的新化合物对应于式I：其中X为卤素原子，含1-4个碳原子的烷基，含1-4个碳原子的烷氧基，甲硫基 基团，甲基磺酰基，二甲基氨磺酰基，三氟甲基或乙酰基; Y是氢，氟或甲基; Z是氧或硫; n为0〜3的整数，R为在1〜4个选自任意酯化的羟基或羟甲基的取代基取代的环中具有4〜6个碳原子的环烷基，甲基，氨基， 乙酰胺基，甲磺酰氨基或氧代基，具有一个或两个选自氧和氮原子并且任选被任选酯化的羟基或氧代基取代的五或六元饱和杂环，任何酯化的羟基是 具有10至22个碳原子的脂族羧酸的酯，以及它们的无毒的药学上可接受的酸加成盐。

    Cyano containing indene derivatives
    6.
    发明授权
    Cyano containing indene derivatives 失效
    含氰基的茚衍生物

    公开(公告)号：US4873344A

    公开(公告)日：1989-10-10

    申请号：US124820

    申请日：1987-11-24

    申请人： Klaus P. Bogeso ,  Michael B. Sommer

    发明人： Klaus P. Bogeso ,  Michael B. Sommer

    IPC分类号： C07C255/47 ,  C07C45/65 ,  C07C45/67 ,  C07C49/617 ,  C07C49/67 ,  C07C49/693 ,  C07C49/697 ,  C07C49/755 ,  C07C62/38 ,  C07C67/00 ,  C07C253/00 ,  C07C253/30 ,  C07C255/45 ,  C07C255/58 ,  C07C311/37 ,  C07C315/04 ,  C07C317/14 ,  C07C317/48 ,  C07C319/20 ,  C07C323/38 ,  C07C323/63 ,  C07D207/32 ,  C07D207/337 ,  C07D207/416 ,  C07D213/57 ,  C07D317/06 ,  C07D317/60 ,  C07D333/24

    CPC分类号： C07D207/337 ,  C07C255/00 ,  C07C45/676 ,  C07C49/697 ,  C07C62/38 ,  C07D213/57 ,  C07D317/60 ,  C07D333/24

    摘要： The present invention relates to novel indene derivatives with the general formula I: ##STR1## wherein R.sup.1 is (a) a phenyl group optionally substituted with one or two groups selected from halogen, lower alkyl, lower alkoxy, lower alkylthio, lower alkylsulfonyl, dilower alkylamino, acylamino such as acetylamino, cyano, trifluoromethyl, trifluoromethoxy, pyrrole and dilower alkylpyrrole,(b) a polycyclic aromatic or heteroaromatic group, such as naphthalene or quinoline,(c) a heteroaromatic group such as thiophene, pyridine, and pyrrole, optionally substituted with one or more groups selected from halogen, lower alkyl, lower alkoxy, lower alkylthio, trifluoromethyl or trifluoromethoxy,R.sub.2 is selected from H, halogen, lower alkyl, benzyl, lower alkylthio, methoxy, lower alkylsulfonyl, dilower alkylsulfamoyl, acylamino such as acetylamino, benzylamino, dilower alkylamino, cyano, pyrrole, dilower alkylpyrrole, trifluoromethyl and trifluoromethoxy,R.sup.3 is CN, COOR.sup.4, --CON(R.sup.4).sub.2 or COR.sup.4, where R.sup.4 is a lower alkyl group, and "n" is an integer of from 1-3 inclusive.The indene derivatives of formula I are, when R.sup.1 is as defined under (a) above, valuable intermediates which are useful in the preparation of pharmacologically effective indane and indene derivatives known from e.g. U.S. Pat. Nos. 4,443,448 and 4,525,360.Moreover, the invention relates to a method for the preparation of the compounds of formula I and to a method for the preparation of compounds of the following formula IV: ##STR2## wherein R.sup.1, R.sup.2 and "n" are as defined above.

    摘要翻译： 本发明涉及具有通式I的新颖的茚衍生物：其中R 1是（a）任选被一个或两个选自卤素，低级烷基，低级烷氧基，低级烷硫基，低级烷基磺酰基， 二氯烷基氨基，酰氨基如乙酰氨基，氰基，三氟甲基，三氟甲氧基，吡咯和二烯烷基吡咯，（b）多环芳族或杂芳族基团如萘或喹啉，（c）杂芳基如噻吩，吡啶和吡咯， 任选被一个或多个选自卤素，低级烷基，低级烷氧基，低级烷硫基，三氟甲基或三氟甲氧基的基团取代，R 2选自H，卤素，低级烷基，苄基，低级烷硫基，甲氧基，低级烷基磺酰基，二低级烷基氨磺酰基， 作为乙酰氨基，苄氨基，二元烷基氨基，氰基，吡咯，二元烷基吡咯，三氟甲基和三氟甲氧基，R3是CN，COOR4，-CON（R4）2或COR4，其中 R4是低级烷基，“n”是1-3的整数。 当R1如上述（a）中所定义时，式I的茚衍生物是有用的中间体，它们可用于制备药物学有效的二氢化茚和茚衍生物，其从例如， 美国专利 第4,443,448号和第4,525,360号。 此外，本发明涉及制备式I化合物的方法和制备下式IV化合物的方法：其中R 1，R 2和“n”如上所定义。

    1,2,3-Triazole and tetrazole substituted piperidine or tetrahydropyridine compounds useful as acetylcholine agonists
    7.
    发明授权
    1,2,3-Triazole and tetrazole substituted piperidine or tetrahydropyridine compounds useful as acetylcholine agonists 失效
    可用作乙酰胆碱激动剂的1,2,3-三唑和四唑取代的哌啶或四氢吡啶化合物

    公开(公告)号：US4866077A

    公开(公告)日：1989-09-12

    申请号：US209994

    申请日：1988-06-22

    申请人： Klaus P. Bogeso ,  Klaus G. Jensen ,  Ejner K. Moltzen ,  Henrik Pedersen

    发明人： Klaus P. Bogeso ,  Klaus G. Jensen ,  Ejner K. Moltzen ,  Henrik Pedersen

    IPC分类号： A61K31/4427 ,  A61K31/445 ,  A61P21/00 ,  A61P25/02 ,  A61P25/28 ,  C07D401/04 ,  C07D413/04 ,  C07D417/04

    CPC分类号： C07D401/04 ,  C07D413/04 ,  C07D417/04

    摘要： The present invention relates to novel compounds of the following formula, where the dotted line designates an optional bond: ##STR1## wherein "het" designates a five membered heterocyclic ring which may include 1 or 2 double bonds and 1-4 heteroatoms selected from nitrogen, oxygen or sulphur, provided that "het" may not designate a 1,2,4- or 1,3,4-oxadiazole;R.sup.1 is selected from hydrogen, lower alkyl, optionally substituted with phenyl which may be substituted with halogen, lower alkyl, or lower alkoxy, or a group R.sup.6 --CO--NH--CH.sub.2 -- or R.sup.6 --O--CO--, wherein R.sup.6 is lower alkyl, branched or unbranched, or phenyl optionally substituted with halogen, trifluoromethyl, lower alkyl, hydroxy, lower alkoxy, or lower acyloxy;R.sup.2 and R.sup.3 are the same or different, each representing hydrogen, lower alkyl, cycloalkyl (3-6 C-atoms), lower alkenyl, lower alkadienyl, lower alkynyl, optionally substituted with hydroxy, halogen or phenyl, in which the phenyl group may be substituted with halogen, trifluoromethyl, lower alkyl, hydroxy or lower alkoxy; R.sup.2 and R.sup.3 may further, respectively, be selected from trifluoromethyl or phenyl optionally substituted with halogen, trifluoromethyl, lower alkyl, hydroxy, lower alkoxy or lower acyloxy, or R.sup.2 and R.sup.3 may, respectively, be a group OR.sup.7 or SR.sup.7 wherein R.sup.7 is defined as R.sup.2 or R.sup.3, andif "het" includes 2 or more carbon atoms, R.sup.4 and R.sup.5 are the same or different, and each is defined as R.sup.2 or R.sup.3, and if "het" includes only one carbon atom, there is only one substituent, R.sup.4, on the heterocyclic ring, and R.sup.4 is defined as R.sup.2 or R.sup.3,as well as individual stereo isomers and pharmaceutically acceptable acid addition salts thereof.The invention moreover relates to methods for the preparation of the compounds of formula I, to novel intermediates, to pharmaceutical compositions containing same and to methods for the treatment of disorders, caused by malfunction of the acetylcholine (AcCh) or muscarinic system, by administering a non-toxic effective amount of a compound of formula I.

    Antihypertensive fluorophenylindanyl imidazolidinoneethylpiperazines
    8.
    发明授权
    Antihypertensive fluorophenylindanyl imidazolidinoneethylpiperazines 失效
    抗高血压氟苯基茚基咪唑烷酮乙基哌嗪

    公开(公告)号：US4684650A

    公开(公告)日：1987-08-04

    申请号：US786199

    申请日：1985-10-10

    申请人： Klaus P. Bogeso

    发明人： Klaus P. Bogeso

    IPC分类号： A61K31/40 ,  A61K31/4015 ,  A61K31/495 ,  A61K31/496 ,  A61K31/505 ,  A61P9/12 ,  A61P25/20 ,  C07D207/24 ,  C07D207/26 ,  C07D207/27 ,  C07D233/36 ,  C07D233/42 ,  C07D235/26 ,  C07D239/22 ,  C07D239/36 ,  C07D239/40 ,  C07D239/96 ,  C07D263/22 ,  C07D403/06 ,  C07D413/06

    CPC分类号： C07D207/26 ,  C07D207/24 ,  C07D233/36 ,  C07D233/42 ,  C07D235/26 ,  C07D239/36 ,  C07D239/40 ,  C07D239/96 ,  C07D263/22

    摘要： The present invention relates to indane derivatives with the following formula: ##STR1## wherein R.sub.1 is H, Halogen, an alkyl group having from one to three carbon atoms inclusive, methoxy, a methylthio-group, or a trifluoromethyl group,n is 2-4X is O or S,Y is O, CH.sub.2 or N--R.sub.2, where R.sub.2 is hydrogen or an (1-6 C) alkyl, (2-6 C) alkenyl or cycloalkyl-methyl group having from three to six carbon atoms,Z is --(CH.sub.2).sub.n --, n is 2 or 3 or Z is 1,2-phenylene optionally substituted with halogen or trifluoromethyl or Z=1,2--C.sub.6 H.sub.4 CO-- (to form a quinazolidinone or -thione ring system). U=N or C.Each compound exists as geometric isomers and each of these as a pair of optical isomers; and the separation and isolation of these are also within the scope of the invention.Moreover, pharmaceutically acceptable acid addition salts of the compounds of Formula I are within the scope of the present invention.Pharmaceutical compositions containing a compound of Formula I or a salt thereof as an active ingredient, and methods for the treatment of hypertension and other cardiovascular diseases as well as anxiety, by administration of a therapeutically active amount of one of the compounds of Formula I to a living animal body, including human beings, fall within the scope of the present invention.

    摘要翻译： 本发明涉及具有下式的二氢化茚衍生物：其中R 1为H，卤素，含有1至3个碳原子的烷基，甲氧基，甲硫基或三氟甲基，其中n为2 -4 X为O或S，Y为O，CH 2或N-R 2，其中R 2为氢或（1-6C）烷基，（2-6C）烯基或具有3-6个碳原子的环烷基 - 甲基 原子，Z是 - （CH 2）n - ，n是2或3或Z是任选被卤素或三氟甲基取代的1,2-亚苯基或Z = 1,2-C 6 H 4 CO-（以形成喹唑啉酮或硫酮环系） 。 U = N或C.每种化合物作为几何异构体存在，它们各自作为一对光学异构体; 并且这些的分离和分离也在本发明的范围内。 此外，式I化合物的药学上可接受的酸加成盐在本发明的范围内。 含有式I化合物或其盐作为活性成分的药物组合物，以及治疗高血压和其它心血管疾病以及焦虑的方法，通过将治疗活性量的一种式I化合物给予 包括人在内的活体动物体属于本发明的范围。

    Xanthene and thioxanthene derivatives, compositions thereof, and treatment therewith
    10.
    发明授权
    Xanthene and thioxanthene derivatives, compositions thereof, and treatment therewith 失效
    呫吨和噻吨衍生物，其组合物及其处理

    公开(公告)号：US4309429A

    公开(公告)日：1982-01-05

    申请号：US105985

    申请日：1979-12-21

    申请人： Niels Lassen ,  Klaus P. Bogeso ,  Peter B. Hansen ,  Jorn L. M. Buus ,  Allan J. Bigler

    发明人： Niels Lassen ,  Klaus P. Bogeso ,  Peter B. Hansen ,  Jorn L. M. Buus ,  Allan J. Bigler

    IPC分类号： C07D409/04 ,  A01N43/40 ,  A61K31/435 ,  A61P25/18 ,  C07D335/16 ,  C07D335/18 ,  C07D405/04 ,  C07D409/06 ,  C07D409/14 ,  C07D413/14 ,  C07D417/04 ,  A61K31/54 ,  A61K31/445

    CPC分类号： C07D335/18 ,  C07C309/00 ,  C07C323/00

    摘要： The present invention relates to novel thioxanthene and xanthene derivatives which have useful pharmacodynamic activity, such as neuroleptic activity and antiemetic activity, methods for the preparation of said derivatives, pharmaceutical compositions containing same, and a method for the treatment of psychic disorders by administering a therapeutically active amount of one of said derivatives to a living animal body, including human beings.The new compounds of the present invention correspond to the Formula I: ##STR1## wherein X is a halogen atom, an alkyl group with from one to four carbon atoms inclusive, an alkyloxy group with from one to four carbon atoms inclusive, a methylthio group, a methylsulphonyl group, a dimethylsulfamoyl group, a trifluoromethyl group or an acetyl group;Y is hydrogen, fluorine or a methyl group;Z is oxygen or sulphur;n is an integer from zero to three inclusive, andR is a cycloalkyl group with from four to six carbon atoms inclusive in the ring substituted with from one to four substituents selected from optionally esterified hydroxy- or hydroxymethyl groups, methyl groups, amino groups, acetamido groups, mesylamino groups or oxo groups, a five- or six-membered saturated heterocyclic ring having one or two heteroatoms selected from oxygen and nitrogen atoms and being optionally substituted with an optionally esterified hydroxy group or oxo group, any esterified hydroxy group present being an ester of an aliphatic carboxylic acid having from ten to twenty-two carbon atoms inclusive, as well as their non-toxic pharmaceutically acceptable acid addition salts.