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1. 发明授权

US4892878A Oleic acid esters and pharmaceutical compositions 失效
标题翻译：油酸酯和药物组合物
公开(公告)号：US4892878A
公开(公告)日：1990-01-09
申请号：US124819
申请日：1987-11-24
申请人： Klaus G. Jensen , Peter Bregnedal
发明人： Klaus G. Jensen , Peter Bregnedal
IPC分类号： C07D279/24 , A61K31/00 , A61K31/445 , A61K31/451 , A61P25/24 , A61P25/26 , A61P43/00 , C07D211/52 , C07D279/28 , C07D335/20 , C07D521/00
CPC分类号： C07D335/20 , C07D211/52 , C07D279/28
摘要： The present invention relates to pharmaceutical compositions of novel oleic acid esters of wellknown neuroleptics and tranquillizers of the phenothiazine, thioxanthene and butyrophenone type containing an aliphatic hydroxy group, and which may be represented by the following general formula: ##STR1## wherein R represents the residue of a hydroxy group containing neuroleptic selected from phenothiazines, thioxanthenes and butyrophenones, as well as pharmaceutically acceptable acid additions salts thereof, which compositions take the form of injectable solutions or suspensions in propylene glycol dioleate (TS-RD-9), methyl oleate or ethyl oleate.None of the esters of Formula I have been specifically described before but have only been broadly disclosed in the patent literature, and the esters as such, as well as a method of preparation of said esters, fall within the scope of the present invention.
摘要翻译：本发明涉及含有脂肪族羟基的吩噻嗪，噻吨酮和丁酰苯胺等众所周知的神经安定药和镇静剂的新型油酸酯的药物组合物，其可以由以下通式表示：其中R表示含有选自吩噻嗪，噻吨酮和丁酰苯的精氨酸的羟基的残基，以及其药学上可接受的酸加成盐，该组合物采用注射溶液或悬浮液形式的丙二醇二油酸酯（TS-RD-9），油酸甲酯或油酸乙酯。式I的酯都没有在前面被具体描述，但是在专利文献中仅被广泛地公开，并且酯本身以及所述酯的制备方法都在本发明的范围内。

2. 发明授权

US4384140A 2-Chloroethyl urea derivatives 失效
标题翻译： 2-氯乙基脲衍生物
公开(公告)号：US4384140A
公开(公告)日：1983-05-17
申请号：US348724
申请日：1982-02-16
申请人： Peter Bregnedal , Jorn L. M. Buus
发明人： Peter Bregnedal , Jorn L. M. Buus
IPC分类号： A61K31/17 , A61K31/275 , A61K31/40 , A61P35/00 , C07C67/00 , C07C239/00 , C07C275/68 , C07C127/17
CPC分类号： C07C275/68
摘要： The present invention relates to novel aminoalkyl substituted nitrosourea derivatives as well as their acid addition salts with pharmaceutically acceptable acids showing pronounced antineoplastic effectiveness in animal experiments.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 and a cyclohexyl group, said phenyl and cyclohexyl groups being optionally substituted with one or two substituents selected from a halogen atom, a lower alkyl group having from one to four carbon atoms inclusive, a trifluore methyl group, a cyano group, a phenyl group, a cyclohexyl group and a lower alkyloxy group having from one to four carbon atoms inclusive."Alkylene" is an alkylene group, branched or unbranched, having from one to four carbon atoms inclusive, 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, and benzyl groups, or they form together with the nitrogen atom a saturated five- or six-membered heterocyclic ring, such as a pyrrolidine, piperidine, morfoline, thiomorfoline, or N-lower-alkyl-piperazine ring, said heterocyclic ring being optionally substituted with lower alkyl groups having from one to four carbon atoms inclusive, as well as pharmaceutically acceptable acid addition salts thereof.
摘要翻译：本发明涉及新的氨基烷基取代的亚硝基脲衍生物及其与药学上可接受的酸的酸加成盐，其在动物实验中显示出明显的抗肿瘤效果。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，并且选自苯基和环己基，所述苯基和环己基任选被一个或两个选自卤素原子，含有1-4个碳原子的低级烷基，三氟甲基，氰基，苯基，环己基和低级烷氧基的取代基取代，一至四个碳原子。 “亚烷基”是具有1〜4个碳原子的支链或非支链的亚烷基，R 1和R 2相同或不同，各自选自具有1〜4个碳原子的低级烷基或者与氮原子一起形成饱和的五元或六元杂环，例如吡咯烷，哌啶，舍弗林，硫代还原或N-低级烷基哌嗪环，所述杂环为任选被具有1至4个碳原子的低级烷基取代，以及其药学上可接受的酸加成盐。

3. 发明授权

US4367239A Nitrosourea derivatives, pharmaceutical compositions thereof and method of preparation 失效
标题翻译：亚硝基脲衍生物，其药物组合物及其制备方法
公开(公告)号：US4367239A
公开(公告)日：1983-01-04
申请号：US191910
申请日：1980-09-29
申请人： Peter Bregnedal , Jorn Buus
发明人： Peter Bregnedal , Jorn Buus
IPC分类号： C07C275/68 , C07C127/17 , A61K31/17
CPC分类号： C07C275/68
摘要： The present invention relates to novel aminoalkyl substituted nitrosourea derivatives as well as their acid addition salts with pharmaceutically acceptable acids showing pronounced antineoplastic effectiveness in animal experiments.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 and a cyclohexyl group, said phenyl and cyclohexyl groups being optionally substituted with one or two substituents selected from a halogen atom, a lower alkyl group having from one to four carbon atoms inclusive, a trifluore methyl group, a cyano group, a phenyl group, a cyclohexyl group and a lower alkyloxy group having from one to four carbon atoms inclusive."Alkylene" is an alkylene group, branched or unbranched, having from one to four carbon atoms inclusive, 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, and benzyl groups, or they form together with the nitrogen atom a saturated five- or six-membered heterocyclic ring, such as a pyrrolidine, piperidine, morfoline, thiomorfoline, or N-lower-alkyl-piperazine ring, said heterocyclic ring being optionally substituted with lower alkyl groups having from one to four carbon atoms inclusive, as well as pharmaceutically acceptable acid addition salts thereof.
摘要翻译：本发明涉及新的氨基烷基取代的亚硝基脲衍生物及其与药学上可接受的酸的酸加成盐，其在动物实验中显示出明显的抗肿瘤效果。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，并且选自苯基和环己基，所述苯基和环己基任选被一个或两个选自卤素原子，含有1-4个碳原子的低级烷基，三氟甲基，氰基，苯基，环己基和低级烷氧基的取代基取代，一至四个碳原子。 “亚烷基”是具有1〜4个碳原子的支链或非支链的亚烷基，R 1和R 2相同或不同，各自选自具有1〜4个碳原子的低级烷基或者与氮原子一起形成饱和的五元或六元杂环，例如吡咯烷，哌啶，舍弗林，硫代还原或N-低级烷基哌嗪环，所述杂环为任选被具有1至4个碳原子的低级烷基取代，以及其药学上可接受的酸加成盐。

4. 发明授权

US3951961A Xanthene and thioxanthene derivatives, compositions thereof and a method of preparation thereof 失效
标题翻译：呫吨和噻吨衍生物，其组合物及其制备方法
公开(公告)号：US3951961A
公开(公告)日：1976-04-20
申请号：US525967
申请日：1974-11-21
申请人： Georg Ujvari , Peter Bregnedal Hansen
发明人： Georg Ujvari , Peter Bregnedal Hansen
IPC分类号： A61K31/395 , C07D311/90 , C07D335/20 , C07D409/06 , C07D405/06
CPC分类号： C07D335/20 , A61K31/395
摘要： The present invention relates to novel xanthene and thioxanthene derivatives of the following general formula: ##SPC1##Wherein Y represents sulfur or oxygen, R.sup.1 represents hydrogen, chlorine, trifluoromethyl or dimethylsulfamoyl, R.sup.2 represents hydrogen or fluorine; and R.sup.3 and R.sup.4 each represents hydrogen or methyl, provided that R.sup.3 and R.sup.4 may not both represent hydrogen, or R.sup.3 and R.sup.4 taken together with the nitrogen atom form a piperazine or piperidine ring optionally substituted in the 4-position by a methyl group or a 2-hydroxyethyl group, if desired, esterified with an aliphatic carboxylic acid having from 1 to 17 carbon atoms inclusive, as well as non-toxic acid addition salts thereof.
摘要翻译：本发明涉及以下通式的新型呫吨和噻吨衍生物：

5. 发明授权

US07351734B2 Aminoindane derivatives as serotonin and norepinephrine uptake inhibitors 失效
标题翻译：氨基茚满衍生物作为5-羟色胺和去甲肾上腺素摄取抑制剂
公开(公告)号：US07351734B2
公开(公告)日：2008-04-01
申请号：US10496730
申请日：2002-12-18
申请人： Klaus Peter Bøgesø , Ask Püschl , Jan Kehler , Peter Bregnedal
发明人： Klaus Peter Bøgesø , Ask Püschl , Jan Kehler , Peter Bregnedal
IPC分类号： A61K31/28 , C07D321/00 , C07D307/00
CPC分类号： A61K31/357 , A61K31/135 , C07C211/42 , C07C2602/08 , C07D317/58 , C07D319/18
摘要： The present invention relates to aminoindane derivatives having the formula I wherein X, Y, U, R1-2, R13-16 and R are as defined in the claims, or an acid addition salt thereof. The compounds of the invention posses the combined effect of serotonin reuptake inhibition and norepinephrine uptake inhibition.
摘要翻译：本发明涉及具有式I的氨基茚满衍生物，其中X，Y，U，R 1-2，R 13-16和R如权利要求中所定义，或其酸加成盐。本发明的化合物具有5-羟色胺再摄取抑制和去甲肾上腺素吸收抑制的综合作用。

6. 发明授权

US06258842B1 Method for the preparation of citalopram 失效
标题翻译：西酞普兰制备方法
公开(公告)号：US06258842B1
公开(公告)日：2001-07-10
申请号：US09564365
申请日：2000-04-28
申请人： Hans Petersen , Peter Bregnedal , Klaus Peter Bogeso
发明人： Hans Petersen , Peter Bregnedal , Klaus Peter Bogeso
IPC分类号： A61K3134
CPC分类号： C07C215/68 , C07C225/22 , C07C233/33 , C07C233/43 , C07D307/87 , C07D307/88
摘要： A method for the preparation of citalopram is described comprising reaction of a compound of Formula (IV) wherein R1 is H or C1-6alkylcarbonyl successively with a Grignard reagent of 4-halogen-fluorophenyl and a Grignard reagent of 3-halogen-N,N-dimethylpropylamine, effecting ring closure of the resulting compound of Formula (IV) and converting the resulting 1,3-dihydroisobenzofuran compound to the corresponding 5-cyano derivative, i.e. citalopram.
摘要翻译：描述了制备西酞普兰的方法，其包括式（Ⅳ）化合物，其中R 1为H或C 1-6烷基羰基，与4-卤代 - 氟苯基的格氏试剂和3-卤素-N，N - 二甲基丙胺，使所得到的式（IV）化合物闭环，并将所得的1,3-二氢异苯并呋喃化合物转化成相应的5-氰基衍生物，即西酞普兰。

7. 发明申请

US20050085530A1 Aminoindane derivatives as serotonin and norepinephrine uptake inhibitors 失效
标题翻译：氨基茚满衍生物作为5-羟色胺和去甲肾上腺素摄取抑制剂
公开(公告)号：US20050085530A1
公开(公告)日：2005-04-21
申请号：US10496730
申请日：2002-12-18
申请人： Klaus Bogeso , Ask Puschl , Jan Kehler , Peter Bregnedal
发明人： Klaus Bogeso , Ask Puschl , Jan Kehler , Peter Bregnedal
IPC分类号： A61K31/135 , A61K31/353 , A61K31/357 , A61K31/36 , A61K31/382 , A61P25/18 , A61P25/22 , A61P25/24 , A61P43/00 , C07C211/42 , C07D317/58 , C07D317/62 , C07D319/18 , C07D335/04
CPC分类号： A61K31/357 , A61K31/135 , C07C211/42 , C07C2602/08 , C07D317/58 , C07D319/18
摘要： The present invention relates to aminoindane derivatives having the formula I wherein X, Y, U, R1-2, R13-16 and R are as defined in the claims, or an acid addition salt thereof. The compounds of the invention posses the combined effect of serotonin reuptake inhibition and norepinephrine uptake inhibition.
摘要翻译：本发明涉及具有式I的氨基茚满衍生物，其中X，Y，U，R 1-2，R 13-16和R如权利要求中所定义，或其酸加成盐。本发明的化合物具有5-羟色胺再摄取抑制和去甲肾上腺素吸收抑制的综合作用。

8. 发明授权

US4022896A Xanthene and thioxanthene compositions and method of treating 失效
标题翻译：呫吨和噻吨酮组合物及其治疗方法
公开(公告)号：US4022896A
公开(公告)日：1977-05-10
申请号：US662331
申请日：1976-03-01
申请人： Georg Ujvari , Peter Bregnedal Hansen
发明人： Georg Ujvari , Peter Bregnedal Hansen
IPC分类号： A61K31/395 , C07D335/20 , A61K31/445
CPC分类号： C07D335/20 , A61K31/395
摘要： The present invention relates to novel xanthene and thioxanthene derivatives of the following general formula: ##STR1## wherein Y represents sulfur or oxygen, R.sup.1 represents hydrogen, chlorine, trifluoromethyl or dimethylsulfamoyl,R.sup.2 represents hydrogen or fluorine; and R.sup.3 and R.sup.4 each represents hydrogen or methyl, provided that R.sup.3 and R.sup.4 may not both represent hydrogen, or R.sup.3 and R.sup.4 taken together with the nitrogen atom form a piperazine or piperidine ring optionally substituted in the 4-position by a methyl group or a 2-hydroxyethyl group, if desired, esterified with an aliphatic carboxylic acid having from one to seventeen carbon atoms inclusive, as well as non-toxic acid addition salts thereof.
摘要翻译：本发明涉及以下通式的新型呫吨和噻吨衍生物：其中Y代表硫或氧，R1代表氢，氯，三氟甲基或二甲基氨磺酰基，R2代表氢或氟; 并且R 3和R 4各自表示氢或甲基，条件是R 3和R 4不能都表示氢，或者R 3和R 4与氮原子一起形成哌嗪或哌啶环，其任选在4-位上被甲基或 2-羟乙基，如果需要，用含有1至17个碳原子的脂族羧酸酯化，以及其无毒的酸加成盐。

9. 发明授权

US5807855A 1-piperazino-1,2-dihydroindene derivatives 失效
标题翻译： 1-哌嗪基-1,2-二氢茚衍生物
公开(公告)号：US5807855A
公开(公告)日：1998-09-15
申请号：US331213
申请日：1994-10-28
申请人： Klaus B.o slashed.ges.o slashed. , Peter Bregnedal
发明人： Klaus B.o slashed.ges.o slashed. , Peter Bregnedal
IPC分类号： C07D241/04 , A61K31/495 , A61P25/00 , A61P25/04 , A61P25/06 , A61P25/16 , A61P25/18 , A61P25/20 , A61P25/22 , A61P25/24 , A61P25/26 , C07D241/38 , C07D295/02 , C07D295/033 , C07D295/073 , C07D333/20 , C07D471/04 , C07D487/04 , C07D409/08
CPC分类号： C07D241/38 , C07D295/033 , C07D295/073 , C07D333/20 , C07D471/04
摘要： Trans isomers of 1-piperazino-1,2-dihydroindene compounds having formula (I), ##STR1## wherein X and Y are hydrogen, halogen, trifluoromethyl, alkyl, alkylthio, trifluoromethylthio, alkoxy, hydroxy, alkylsulfonyl, amino, alkylamino, nitro or cyano; Ar is a phenyl, thienyl or furyl group, each optionally substituted; R.sub.1 is hydrogen, or optionally hydroxy substituted alkyl, alkenyl, cycloalkyl or cycloalkylalkyl; R.sub.2 is alkyl, alkenyl, cycloalkyl, or cycloalkylalkyl; or R.sub.1 and R.sub.2 together form a 5 to 7-membered heterocyclic ring fused with the piperazine ring, which ring may be substituted with hydroxy; R.sub.3 is hydrogen, alkyl, alkenyl, cycloalkyl or cycloalkylalkyl; or R.sub.2 and R.sub.3 together form a 3 to 7-membered carbocyclic ring which is spiro-fused to the piperazine ring; and R.sub.4 is hydrogen or alkyl. The compounds of the invention have potent antagonist action on dopamine D.sub.1 receptors and are useful in the treatment of diseases of the central nervous system, such as psychoses, schizophrenia (positive as well as negative symptoms), anxiety, depression, sleep disturbances, migraine, Parkinson's disease or cocaine abuse.
摘要翻译：具有式（I）的1-哌嗪基-1,2-二氢茚化合物的反式异构体，其中X和Y是氢，卤素，三氟甲基，烷基，烷硫基，三氟甲硫基，烷氧基，羟基，烷基磺酰基，氨基，烷基氨基，硝基或氰基; Ar是苯基，噻吩基或呋喃基，各自任选被取代; R 1是氢或任选的羟基取代的烷基，烯基，环烷基或环烷基烷基; R2是烷基，烯基，环烷基或环烷基烷基; 或者R 1和R 2一起形成与哌嗪稠合的5至7元杂环，该环可以被羟基取代; R3是氢，烷基，烯基，环烷基或环烷基烷基; 或者R 2和R 3一起形成与哌嗪环螺稠合的3至7元碳环; 和R4是氢或烷基。本发明的化合物对多巴胺D1受体具有有效的拮抗剂作用，可用于治疗中枢神经系统疾病，如精神病，精神分裂症（阳性和阴性症状），焦虑症，抑郁症，睡眠障碍，偏头痛，帕金森病或可卡因滥用。

10. 发明授权

US5643784A Indan derivatives 失效
标题翻译：印度衍生品
公开(公告)号：US5643784A
公开(公告)日：1997-07-01
申请号：US383708
申请日：1995-02-01
申请人： Klaus P. B.o slashed.ges.o slashed. , Peter Bregnedal
发明人： Klaus P. B.o slashed.ges.o slashed. , Peter Bregnedal
IPC分类号： C07D207/24 , C07D207/26 , C07D207/263 , C07D233/36 , C07D233/42 , C07D235/26 , C07D239/10 , C07D263/22 , A61K31/495 , A61K31/505 , C07D403/06 , C07D413/06
CPC分类号： C07D207/263 , C07D207/24 , C07D233/36 , C07D233/42 , C07D235/26 , C07D239/10 , C07D263/22
摘要： The subject invention relates to 5-Substituted trans-1-piperazinoindan derivatives having general formula (I), ##STR1## wherein X is halogen, trifluromethyl, alkyl, alkylthio, alkyloxy, hydroxy, alkylsulphonyl, alkyl- or dialkylamino, triflouromethylthio or cyano; R is hydrogen, or alkyl, alkenyl, cycloalkyl, cycloalkyl lower alkyl, optionally substituted with hydroxy, or R is a substituent, ##STR2## wherein n is an integer from 1 to 6; U is CH or N; Y is, CH.sub.2, O, S or N-R.sup.1, R.sup.1 being hydrogen or cycloalkyl, cycloalkylmethyl, alkyl or alkenyl optionally substituted with hydroxy or an optionally substituted phenyl group; W is O or S; Z is --(CH.sub.2).sub.4 --, ##STR3## where R.sup.2 and R.sup.3 are hydrogen or lower alkyl, --CH.dbd.CH--, --CH.dbd.CH--CH.sub.2 --, optionally substituted 1,2-phenylene, 1,2-C.sub.6 H.sub.4 CH.sub.2 -- (to form a quinazolidinone or -thione ring system) or 1,2-C.sub.6 H.sub.4 CO-- (to form a quinazolidindion or thixoquinazolidinon ring system); and Ar is an optionally substituted phenyl, thiophene or furane ring; are selective, centrally acting 5-HT.sub.2 antagonists useful in the treatment of anxiety, depression, sleeping disorders, negative symptoms of schizophrenia and migraine.
摘要翻译：本发明涉及具有通式（I）的5-取代的反式-1-哌嗪基茚满代衍生物，其中X是卤素，三氟甲基，烷基，烷硫基，烷氧基，羟基，烷基磺酰基，烷基 - 或二烷基氨基，三氟甲硫基或氰基; R是氢或任选被羟基取代的烷基，烯基，环烷基，环烷基低级烷基，或R是取代基，其中n是1至6的整数; U是CH或N; Y是，CH2，O，S或N-R1，R1是氢或环烷基，环烷基甲基，任选被羟基或任选取代的苯基取代的烷基或链烯基; W为O或S; Z是 - （CH 2）4 - ，其中R 2和R 3是氢或低级烷基，-CH = CH-，-CH = CH-CH 2 - ，任选取代的1,2-亚苯基，1,2-C 6 H 4 CH 2 - （形成喹唑啉酮或硫酮环系）或1,2--C 6 H 4 CO-（形成喹唑啉基或噻唑烷环酮系）; 并且Ar是任选取代的苯基，噻吩或呋喃环; 是选择性的中枢作用的5-HT2拮抗剂，可用于治疗焦虑，抑郁，睡眠障碍，精神分裂症和偏头痛的阴性症状。

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