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21. 发明申请

US20080108645A1 Dihydrotetrabenazines And Pharmaceutical Compositions Containing Them 审中-公开
标题翻译：二氢四苯并嗪及其药物组合物
公开(公告)号：US20080108645A1
公开(公告)日：2008-05-08
申请号：US10597803
申请日：2005-02-11
申请人： Robert Tridgett , Ian Clarke , Robert Turtle , Grant Johnston
发明人： Robert Tridgett , Ian Clarke , Robert Turtle , Grant Johnston
IPC分类号： A61K31/4375 , A61P25/00 , C07D455/06 , C07D491/147
CPC分类号： C07D455/06 , C07D471/04 , C07D491/14
摘要： The invention provides novel isomers of dihydrotetrabenazine, individual enantiomers and mixtures thereof wherein the dihydrotetrabenazine is a 3,11 b-cis-dihydrotetrabenazine. Also provided are methods for the preparation of the novel isomers, pharmaceutical compositions containing them and their use in treating hyperkinetic movement disorders such as Huntington's disease, hemiballismus, senile chorea, tic, tardive dyskinesia and Tourette's syndrome.
摘要翻译：本发明提供二氢丁苯那嗪的新异构体，单独的对映异构体及其混合物，其中二氢丁苯那嗪是3,11b-顺 - 二氢丁苯那嗪。还提供了制备新异构体的方法，含有它们的药物组合物及其用于治疗运动过度运动障碍如亨廷顿舞蹈病，半血糖症，老年性舞蹈病，抽搐，迟发性运动障碍和图雷特综合征的用途。

22. 发明申请

US20080076925A1 PROCESS FOR THE PREPARATION OF PYRIDO [ 2-1-A] ISOQUINOLINE DERIVATIVES BY CATALYTIC ASYMMETRIC HYDROGENATION OF AN ENAMINE 审中-公开
标题翻译：制备吡啶的方法[
公开(公告)号：US20080076925A1
公开(公告)日：2008-03-27
申请号：US11853119
申请日：2007-09-11
申请人： Stefan Abrecht , Michelangelo Scalone , Rudolf Schmid
发明人： Stefan Abrecht , Michelangelo Scalone , Rudolf Schmid
IPC分类号： C07D455/06
CPC分类号： C07D455/06 , B01J31/2295 , B01J2231/641 , B01J2531/822 , C07D471/04 , Y02P20/55
摘要： The invention relates to a process for the preparation of pyrido[2,1-a] isoquinoline derivatives of the formula wherein R2, R3and R4 are as defined in the specification, comprising the steps of a) catalytic asymmetric hydrogenation of an enamine of the formula wherein R1 is lower alkyl, in the presence of a transition metal catalyst containing a chiral diphosphane ligand, b) introduction of an amino protecting group Prot and c) amidation of the ester to form an amide of formula wherein R2, R3, R4 and Prot are as defined in the specification.
摘要翻译：本发明涉及制备下式的吡啶并[2,1-a]异喹啉衍生物的方法，其中R 2，R 3和R 4， / SUP>如说明书中所定义，包括以下步骤：a）在含有手性的过渡金属催化剂存在下，催化不对称氢化下式的烯胺，其中R 1是低级烷基二膦配体，b）引入氨基保护基团Prot和c）酯的酰胺化形成下式的酰胺，其中R 2，R 3，R 3， 4和Prot如说明书中所定义。

23. 发明申请

US20050221213A1 Hydrazone-based charge transport materials 失效
标题翻译：腙类电荷输送材料
公开(公告)号：US20050221213A1
公开(公告)日：2005-10-06
申请号：US10815243
申请日：2004-03-31
申请人： Nusrallah Jubran , Zbigniew Tokarski , Vytautas Getautis , Maryte Daskeviciene , Tadas Malinauskas , Jonas Sidaravicius , Vygintas Jankauskas
发明人： Nusrallah Jubran , Zbigniew Tokarski , Vytautas Getautis , Maryte Daskeviciene , Tadas Malinauskas , Jonas Sidaravicius , Vygintas Jankauskas
IPC分类号： G03G5/04 , C07C251/86 , C07D209/86 , G03G5/047 , G03G5/06 , C07D209/82 , C07D455/06
CPC分类号： G03G5/0614 , C07C251/86 , C07D209/86 , G03G5/0616 , G03G5/0618 , G03G5/062 , G03G5/0629
摘要： Improved organophotoreceptor comprises an electrically conductive substrate and a photoconductive element on the electrically conductive substrate, the photoconductive element comprising: (a) a charge transport material having the formula where R1, R2, R3, R4, R5, R6, R7, and R8, are, each independently, an alkyl group, an alkenyl group, an alkynyl group, an aryl group, or a heterocyclic group; R9 and R10 are, each independently, H, an alkyl group, an alkenyl group, an alkynyl group, an aryl group, or a heterocyclic group; Ar1 and Ar2 are, each independently, an aromatic group; Y is an arylamine group; and X1 and X2 are, each independently, a linking group; and (b) a charge generating compound. Corresponding electrophotographic apparatuses and imaging methods are described.
摘要翻译：改进的有机光感受器包括在导电衬底上的导电衬底和光电导元件，光电导元件包括：（a）具有下式的电荷传输材料：其中R 1，R 2， R 3，R 3，R 4，R 5，R 6，R 7， R 3和R 8各自独立地为烷基，烯基，炔基，芳基或杂环基; R 9和R 10各自独立地为H，烷基，烯基，炔基，芳基或杂环基; Ar 1和Ar 2各自独立地为芳族基团; Y是芳基胺基; 和X 1和X 2各自独立地为连接基团; 和（b）电荷产生化合物。描述相应的电子照相设备和成像方法。

24. 发明授权

US5723633A Pyran derivative, photosensitive resin composition, and hologram recording medium using it 失效
公开(公告)号：US5723633A
公开(公告)日：1998-03-03
申请号：US575387
申请日：1995-12-20
申请人： Shin Kobayashi , Susumu Matsumura , Naosato Taniguchi , Yoko Yoshinaga , Toshiyuki Sudo , Hideki Morishima , Tadashi Kaneko
发明人： Shin Kobayashi , Susumu Matsumura , Naosato Taniguchi , Yoko Yoshinaga , Toshiyuki Sudo , Hideki Morishima , Tadashi Kaneko
IPC分类号： C07D209/04 , C07D309/34 , C07D315/00 , C07D455/04 , C07D455/06 , C08F2/50 , G03F7/028 , G03F7/031 , G03H1/02
CPC分类号： G03H1/02 , C07D309/34 , C07D455/04 , G03H2001/0264
摘要： A pyran derivative has a structure of R.sup.2 R.sup.3 C.dbd.(C.sub.5 H.sub.2 R.sup.1 O)--(CH.dbd.CH).sub.n --C.sub.6 H.sub.2 R.sup.6 R.sup.7 --NR.sup.4 R.sup.5 wherein n is 3 or 4; R.sup.1 is a proton, alkyl or phenyl group; each of R.sup.2 and R.sup.3 is independently a cyano, alkoxycarbonyl having an alkyl, acyl having an alkyl, aracyl having phenyl, sulfonyl, aryl, or aryloxy; each of R.sup.4 and R.sup.5 is an alkyl group; and each of R.sup.6 and R.sup.7 is a proton, provided that R.sup.4 and R.sup.5 are alkyl groups, and a pair of R.sup.4 and R.sup.6 as well as a pair of R.sup.5 and R.sup.7 can be bonded to each other to form a heterocycle. A photosensitive composition comprises a polymerizable compound, a polymerization initiator and a photosensitizer which is the pyran derivative. A photosensitive resin composition comprises a crosslinkable polymer, a crosslinking agent and the photosensitizer. A hologram recording medium mainly comprises the photosensitive composition or the photosensitive resin composition.

25. 发明授权

US5561233A Process for the preparation of an intermediate of a benzo[a]quinolizinone derivative 失效
标题翻译：制备苯并[a]喹嗪酮衍生物的中间体的方法
公开(公告)号：US5561233A
公开(公告)日：1996-10-01
申请号：US452793
申请日：1995-05-30
申请人： Paul Spurr
发明人： Paul Spurr
IPC分类号： A61K31/435 , A61P25/20 , C07D455/06
CPC分类号： C07D455/06
摘要： The invention is concerned with a process for the preparation of a benzo[a]quinolizinone derivative of the formula ##STR1## by reacting a compound of the formula ##STR2## wherein X is halogen and Ph is phenyl, with carbon monoxide in the presence of a carbonylation catalyst and in the presence of (S)-3-ethoxypyrrolidine or a lower alkanol or water; where a lower alkyl ester of the 10-chloro-6,7-dihydro-4 -oxo-3-phenyl-4H-benzo[a]quinolizine-1-carboxylic acid has been obtained, converting this into the corresponding free acid; and, where the 10-chloro-6,7-dihydro-4-oxo-3-phenyl-4H-benzo[a]quinolizine-1-carboxylic acid has been obtained, reacting a reactive derivative thereof with (S)-3-ethoxypyrrolidine. The compound of formula I is useful for the treatment or prophylaxis of sleep disorders.
摘要翻译：本发明涉及制备式I的苯并[a]喹嗪酮衍生物的方法，其中式Ⅰ的化合物其中X为卤素且Ph为苯基的式Ⅰbb与一氧化碳在在（S）-3-乙氧基吡咯烷或低级链烷醇或水的存在下，存在羰基化催化剂; 其中得到10-氯-6,7-二氢-4-氧-3-苯基-4H-苯并[a]喹嗪-1-羧酸的低级烷基酯，将其转化为相应的游离酸; 并且其中已经获得了10-氯-6,7-二氢-4-氧代-3-苯基-4H-苯并[a]喹嗪-1-羧酸，使其反应性衍生物与（S）-3- 乙氧基吡咯烷。式I化合物可用于治疗或预防睡眠障碍。

26. 发明授权

US5281711A (S)-1-[10-chloro-6,7-dihydro-4-oxo-3-phenyl-4H-benzo[a]quino-lizin-1-yl) carbonyl]-3-ethoxypyrrolidine 失效
标题翻译：（S）-1- [10-氯-6,7-二氢-4-氧代-3-苯基-4H-苯并[a]喹喔啉-1-基）羰基] -3-乙氧基吡咯烷
公开(公告)号：US5281711A
公开(公告)日：1994-01-25
申请号：US818653
申请日：1992-01-06
申请人： Richard R. Scherschlicht , Ulrich Widmer
发明人： Richard R. Scherschlicht , Ulrich Widmer
IPC分类号： A61K31/47 , A61K31/4025 , A61K31/435 , A61K31/4375 , A61P25/20 , C07D207/12 , C07D401/14 , C07D455/04 , C07D455/06 , C07D471/04 , A61F13/02 , A61K9/28 , A61K9/48
CPC分类号： C07D455/06 , Y10S424/15 , Y10S514/923
摘要： The compound (S)-1-[(10-chloro-6,7-dihydro-4-oxo-3-phenyl-4H-benzo[a]quino-lizin-1-yl)carbonyl]-3-ethoxypyrrolidine of the formula ##STR1## which has valuable pharmacological properties, is described. In particular, the compound of formula I has a non-sedating, hypnotic, that is, sleep-promoting, activity and can accordingly be used for the treatment of sleep disorders.
摘要翻译：化合物（S）-1 - [（10-氯-6,7-二氢-4-氧代-3-苯基-4H-苯并[a]喹喔啉-1-基）羰基] -3-乙氧基吡咯烷具有有价值的药理性质的公式 I描述。特别地，式I化合物具有非镇静，催眠，即睡眠促进活性，因此可用于治疗睡眠障碍。

27. 发明授权

US5278308A Iodine derivatives of tetrabenazine 失效
标题翻译：丁苯那酸的碘衍生物
公开(公告)号：US5278308A
公开(公告)日：1994-01-11
申请号：US843041
申请日：1992-02-28
申请人： Hank F. Kung
发明人： Hank F. Kung
IPC分类号： C07D455/06
CPC分类号： C07D455/06
摘要： Compounds of the formula ##STR1## where R.sub.1 and R.sub.2 are independently selected from the group consisting of H, OH, OCH.sub.3, and Halogen or R.sub.1 and R.sub.2 can be taken together to form --O--CH.sub.2 --O--;R.sub.3 and R.sub.4 are independently selected from the group consisting of H, OH, C.sub.1 -C.sub.10 alkyl, C.sub.1 -C.sub.10 alkoxy, C.sub.1 -C.sub.10 alkenyloxy, --R.sub.7 --CH.dbd.CHI, and ##STR2## n is an integer from 0 to 5; X and Y are independently selected from the group consisting of H, OH, OCH.sub.3, Halogen and --R.sub.7 --CH.dbd.CHI;R.sub.5 and R.sub.6 are independently selected from the group consisting of H, OH, C.sub.1 -C.sub.10 alkyl, C.sub.1 -C.sub.10 alkoxy, C.sub.1 -C.sub.10 alkenyloxy, --R.sub.7 --CH.dbd.CHI, --CONR.sub.8 R.sub.9 and ##STR3## X' and Y' are independently selected from the group consisting of H, OH, OCH.sub.3, Halogen, and --R.sub.7 --CH.dbd.CHI;R.sub.7 is selected from the group consisting of a chemical bond and C.sub.1 -C.sub.10 alkyl; andR.sub.8 and R.sub.9 are independently selected from the group consisting of H and C.sub.1 -C.sub.10 alkyl;provided that there is at least one iodine atom directly attached to a phenyl moiety or as part of a --CH.dbd.CHI moiety in one or more substituents selected from the group consisting of R.sub.3, R.sub.4, R.sub.5 and R.sub.6 are disclosed as being useful as imaging agents for evaluation of the central nervous system neuronal system.
摘要翻译：其中R 1和R 2独立地选自H，OH，OCH 3和卤素或R 1和R 2的式的化合物可一起形成-O-CH 2 -O-; R 3和R 4独立地选自H，OH，C 1 -C 10烷基，C 1 -C 10烷氧基，C 1 -C 10链烯氧基，-R 7 -CH = CHI，且n为0至5的整数; X和Y独立地选自H，OH，OCH 3，卤素和-R 7 -CH = CHI; R 5和R 6独立地选自H，OH，C 1 -C 10烷基，C 1 -C 10烷氧基，C 1 -C 10链烯氧基，-R 7 -CH = CH 1，-CONR 8 R 9和X'和Y'独立地选自由H，OH，OCH 3，卤素和-R 7 -CH = CHI组成的组; R7选自化学键和C1-C10烷基; 并且R 8和R 9独立地选自H和C 1 -C 10烷基; 条件是在一个或多个选自R3，R4，R5和R6的取代基中存在至少一个碘原子直接连接到苯基部分或作为-CH = CHI部分的一部分，其被公开用作成像用于评估中枢神经系统神经元系统的药剂。

28. 发明授权

US4889848A Tricyclic pyridine derivatives 失效
公开(公告)号：US4889848A
公开(公告)日：1989-12-26
申请号：US141022
申请日：1988-01-05
申请人： Ulf Fischer , Fernand Schneider , Ulrich Widmer
发明人： Ulf Fischer , Fernand Schneider , Ulrich Widmer
IPC分类号： C07D205/04 , C07D333/38 , C07D455/02 , C07D455/06 , C07D495/04 , C07D495/14 , C07D513/04 , C07D513/14 , C07D513/18 , C07D513/22 , C07D519/00
CPC分类号： C07D495/04 , C07D205/04 , C07D333/38 , C07D455/02 , C07D455/06 , C07D495/14 , C07D513/04 , C07D513/14
摘要： Compounds of the formula ##STR1## wherein Q.sup.1 and the nitrogen atom taken together are a group of the formula >N--CH.sub.2 CH.sub.2 -- (a), >N--CH.sub.2 CH.sub.2 CH.sub.2 -- (b), >N--CH.dbd.CH-- (c), >N--CH.sub.2 --CH.dbd.CH-- (d), >N--CH.sub.2 --S(O).sub.p -- (e), >N--CH.sub.2 CH.sub.2 --S(O).sub.p -- (f) or >N--CH.dbd.CH--S(O).sub.p -- (g), p is the integer 0, 1 or 2, Ra is a phenyl, pyridyl or thienyl group which is optionally substituted by halogen, trifluoromethyl, nitro, lower alkyl or lower alkoxy, Rb and Rc each, independently, are hydrogen, halogen, trifluoromethyl, lower alkyl, lower alkoxy or nitro and the dotted line signifies an optional bond, or Rb and Rc together with the carbon atom denoted by .alpha. are a group of the formula >C.alpha.--S--CH.dbd.CH-- (h), >C.alpha.--CH.dbd.CH--S-- (i) or >C.alpha.--CH.dbd.CH--CH.dbd.CH-- (j) which is optionally substituted by halogen, trifluoromethyl, lower alkyl, lower alkoxy, nitro, amino or mono- or di(lower alkyl)amino, and the dotted line signifies an additional bond, Rd is the group of the formula --(A.sup.1).sub.m --(CO).sub.n --(Q.sup.2 A.sup.2).sub.q --R.sup.1, m, m and q each, independently, are the integer 0 or 1, A.sup.1 is lower alkylene, A.sup.2 is lower alkylene, a direct bond or the group --CO--, Q.sup.2 is an oxygen atom or the group --NR.sup.2 --, R.sup.1 is hydrogen, hydroxy, cyano, nitro, halogen, lower alkoxy, lower alkyl, lower alkoxycarbonyl, aryl, a group of the formula --NR.sup.3 R.sup.4 or a 5-membered, saturated, partially unsaturated or aromatic heterocycle which is attached via a carbon atom and which is optionally substituted by one or two lower alkyl groups and optionally substituted by a (C.sub.3-6)-cycloalkyl, hydroxy, lower alkoxy, lower alkanoyloxy, lower hydroxyalkyl, lower alkoxyalkyl, lower alkanoyloxyalkyl, lower alkoxycarbonyl, lower alkanoyl, carbamoyl, mono- or di(lower alkyl)carbamoyl, oxo or alkylenedioxy group, R.sup.2 is hydrogen, lower alkyl or aryl, R.sup.3 and R.sup.4 each, independently, are hydrogen, lower alkyl, lower alkoxyalkyl, lower dialkoxyalkyl, lower alkylenedioxyalkyl, lower cyanoalkyl, lower haloalkyl, lower hydroxyalkyl, lower dihydroxyalkyl, lower alkanoyl, lower alkoxycarbonyl or a (C.sub.3-7)-cycloalkyl group which is optionally substituted by hydroxy, lower alkoxy, lower alkanoyloxy, lower hydroxyalkyl, lower alkoxyalkyl, lower alkanoyloxyalkyl, oxo, carbamoyl, mono- or di(lower alkyl)carbamoyl or by lower alkylenedioxy or together with the nitrogen atom is a 3- to 7-membered, saturated N-heterocycle which is optionally substituted by one or two lower alkyl groups and optionally substituted by one or two hydroxy, lower alkoxy, lower alkanoyloxy, lower hydroxyalkyl, lower alkoxyalkyl, lower alkanoyloxyalkyl, lower alkoxycarbonyl, lower alkanoyl, carbamoyl, mono- or di(lower alkyl)carbamoyl, oxo or lower alkylenedioxy groups and which can contain as a ring member an oxygen or sulfur atom or the group >N--R.sup.5, and R.sup.5 is hydrogen, lower alkyl, lower hydroxyalkyl, lower alkoxyalkyl, lower alkanoyloxyalkyl, lower alkanoyl, lower alkoxycarbonyl, carbamoyl or mono- or di(lower alkyl) carbamoyl, with the proviso that n is 0 when q is 1 and A.sup.2 is the group --CO--, that R.sup.1 is other than cyano, nitro, halogen or lower alkoxycarbonyl when q is 0 and n is 1 or when q is 1 and A.sup.2 is --CO--, and that R.sup.1 is other than hydroxy, cyano, nitro, halogen, lower alkoxycarbonyl, lower alkoxy and --NR.sup.3 R.sup.4 when q is 1 and A.sup.2 is a direct bond,or a pharmaceutically acceptable acid addition salt of a compound of formula I which has one or more basic substituents, are described.The compounds of formula I possess pronounced muscle relaxant, sedative-hypnotic, anticonvulsive and anxiolytic properties and have low toxicity.

29. 发明授权

US4650804A Quinolizinone compounds and pharmaceutical composition comprising the same, useful as anti-ulcerative and anti-allergic agents 失效
标题翻译：喹诺酮类化合物和包含其的药物组合物，可用作抗溃疡和抗过敏剂
公开(公告)号：US4650804A
公开(公告)日：1987-03-17
申请号：US712435
申请日：1985-03-18
申请人： Yoshihiko Kitaura , Teruo Oku , Hideo Hirai , Tosiyuki Yamamoto , Masashi Hashimoto
发明人： Yoshihiko Kitaura , Teruo Oku , Hideo Hirai , Tosiyuki Yamamoto , Masashi Hashimoto
IPC分类号： A61K31/435 , A61K31/47 , A61P1/04 , A61P37/08 , A61P43/00 , C07D455/00 , C07D455/02 , C07D455/03 , C07D455/04 , C07D455/06 , C07F7/18 , C07D221/06 , C07D239/02
CPC分类号： C07D455/00 , C07D455/02 , C07D455/04 , C07D455/06 , C07F7/1856 , Y02P20/55
摘要： The invention relates to novel quinolizinone compounds having inhibitory activity on allergies and ulcers, of the formula: ##STR1## wherein R.sup.1 is tetrazolylcarbamoyl;R.sup.7 is hydrogen or aryl selected from phenyl, tolyl, xylyl, cumenyl, naphthyl and biphenylyl;R.sup.2 is hydrogen, hydroxy, lower alkyl or lower alkoxy;R.sup.3 is hydrogen, hydroxy, lower alkyl, lower alkoxy, lower alkenyloxy, phenyl, napthyl, biphenylyl, phenyl having one or more substituent(s) selected from halogen, lower alkyl and lower alkoxy, arylthio selected from phenylthio, tolylthio, xylylthio, cumenylthio, naphthylthio and biphenylthio, aroyl selected from benzoyl, toluoyl and naphthoyl, ar(lower)alkyl selected from phenyl(lower)alkyl, tolyl(lower)alkyl, xylyl(lower)alkyl, cumenyl(lower)alkyl, naphthyl(lower)alkyl and biphenylyl(lower)alkyl, arenesulfonyl selected from benzenesulfonyl and p-toluenesulfonyl, arylamino selected from phenylamino, naphthylamino, biphenylylamino, phenylamino having lower alkyl on the nitrogen atom or aryloxy selected from phenoxy and tolyloxy;or pharmaceutically acceptable salts thereof.
摘要翻译：本发明涉及具有下式的过敏和溃疡抑制活性的新型喹嗪酮化合物：其中R1是四唑基氨基甲酰基; R7是氢或选自苯基，甲苯基，二甲苯基，枯烯基，萘基和联苯基的芳基; R2是氢，羟基，低级烷基或低级烷氧基; R3是氢，羟基，低级烷基，低级烷氧基，低级烯氧基，苯基，萘基，联苯基，具有一个或多个选自卤素，低级烷基和低级烷氧基的取代基的苯基，选自苯硫基，甲苯硫基，二甲苯硫基，，萘基硫基和联苯硫基，选自苯甲酰基，甲苯酰基和萘甲酰基的芳酰基，选自苯基（低级）烷基，甲苯基（低级）烷基，二甲苯基（低级）烷基，枯烯基（低级）烷基，萘基和选自苯磺酰基和对甲苯磺酰基的联苯基（低级）烷基，芳基磺酰基，选自苯基氨基，萘基氨基，联苯基氨基，在氮原子上具有低级烷基的苯基氨基或选自苯氧基和甲酰基氧基的芳氧基; 或其药学上可接受的盐。

30. 发明授权

US4604398A Benzoquinolizine derivatives, and their use as .alpha..sub.2 adrenoceptor antagonistic agents 失效
标题翻译：苯醌喹啉衍生物及其作为α2肾上腺素受体拮抗剂的用途
公开(公告)号：US4604398A
公开(公告)日：1986-08-05
申请号：US744843
申请日：1985-06-13
申请人： Terence J. Ward
发明人： Terence J. Ward
IPC分类号： C07D455/06 , A61K31/435
CPC分类号： C07D455/06
摘要： The invention concerns benzoquinolizines of general formula ##STR1## or their pharmaceutically acceptable acid addition salts. In the formula R.sup.1 and R.sup.2 which may be the same or different each represent hydrogen, lower alkyl, lower alkoxy or halogen, R.sup.3 represents lower alkyl and R.sup.4 is lower alkoxy or lower alkoxy carbonyl. The compounds possess .alpha..sub.2 -adrenoceptor antagonistic activity in warm blooded animals.
摘要翻译：本发明涉及通式为（I）的苯喹啉或其药学上可接受的酸加成盐。在式中，R 1和R 2可以相同或不同，各自表示氢，低级烷基，低级烷氧基或卤素，R 3表示低级烷基，R 4是低级烷氧基或低级烷氧基羰基。该化合物在温血动物中具有α2-肾上腺素受体拮抗作用。

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