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41. 发明授权

US06372780B1 Methods of treating cell lines expressing multidrug resistance P-glycoprotein 有权
公开(公告)号：US06372780B1
公开(公告)日：2002-04-16
申请号：US09752779
申请日：2001-01-03
申请人： Hervé Bouchard , Jean-Dominique Bourzat , Alain Commerçon
发明人： Hervé Bouchard , Jean-Dominique Bourzat , Alain Commerçon
IPC分类号： A61K31337
摘要： Now taxoids of general formula (I) their preparation and pharmaceutical compositions containing them. The new products of general formula (I) in which Z represents a radical of general formula (II): display noteworthy antitumor and antileukaemic properties.

42. 发明授权

US06331635B1 Taxoids, their preparation and pharmaceutical compositions containing them 失效
标题翻译：紫杉烷类，它们的制备方法和含有它们的药物组合物
公开(公告)号：US06331635B1
公开(公告)日：2001-12-18
申请号：US09066929
申请日：1998-04-28
申请人： Hervé Bouchard , Jean-Dominique Bourzat , Alain Commerçon
发明人： Hervé Bouchard , Jean-Dominique Bourzat , Alain Commerçon
IPC分类号： C07D26306
CPC分类号： C07D305/14 , Y02P20/55
摘要： New taxoids of general formula (I): their preparation and pharmaceutical compositions containing them. The new products of general formula (I) in which Z represents a radical of general formula (II): display noteworthy antitumour and antileukaemic properties.
摘要翻译：通式（I）的新紫杉烷类：它们的制备方法和含有它们的药物组合物。其中Z代表通式（II）的基团的通式（I）的新产品：显示出显着的抗肿瘤和抗白血病性质。

43. 发明授权

US06218406B1 Farnesyl transferase inhibitors, their preparation, the pharmaceutical compositions which contain them and their use in the preparation of medicaments 失效
标题翻译：法呢基转移酶抑制剂，它们的制备，含有它们的药物组合物及其在制备药物中的用途
公开(公告)号：US06218406B1
公开(公告)日：2001-04-17
申请号：US09346303
申请日：1999-07-02
申请人： Jean-Dominique Bourzat , Alain Commerçon , Norbert Dereu , Patrick Mailliet , Fabienne Sounigo-Thompson , Jean-Paul Martin , Marc Capet , Michel Cheve
发明人： Jean-Dominique Bourzat , Alain Commerçon , Norbert Dereu , Patrick Mailliet , Fabienne Sounigo-Thompson , Jean-Paul Martin , Marc Capet , Michel Cheve
IPC分类号： A61K314439
CPC分类号： C07D401/12 , C07D209/56 , C07D209/72 , C07D403/04 , C07D405/04 , C07D405/14 , C07D409/04 , C07D409/12 , C07D409/14
摘要： Novel products of formula (I), their preparation, the pharmaceutical compositions which contain them and their use in the preparation of medicaments. In the formula (I), the following substituents are among the preferred: Ar represents a substituted or condensed phenyl radical or a polycyclic or heterocyclic aromatic radical, R represents a radical of general formula —(CH2)m—X1—(CH2)n—Z in which X1=single bond, O, S; m=0, 1; n=0, 1, 2; it being possible for the CH2 radicals to be substituted; Z represents carboxyl, COOR6 (R6=alkyl), CON(R7)(R8) (R7=hydrogen or alkyl and R8=hydrogen, hydroxyl, arylsulphonyl, heterocyclyl, optionally substituted amino, optionally substituted alkyloxy or optionally substituted alkyl), PO(OR9)2 (R9=hydrogen or alkyl), an —NH—CO—T (T=hydrogen or optionally substituted alkyl) radical, or else—a radical, R1 and R2=hydrogen or halogen or alkyl, alkyloxy, which is optionally substituted, alkylthio, alkyloxycarbonyl or else R1 and R2, at the ortho position with respect to one another, form an optionally substituted heterocycle containing 1 or 2 heteroatoms, R3 and R4=hydrogen or halogen or alkyl, alkenyl, alkyloxy, alkylthio, carboxyl or alkyloxycarbonyl, R5=hydrogen, alkyl, alkylthio, X=O or S or —NH—, —CO—, methylene, vinyldiyl, alkene-1,1-diyl or cycloalkane-1,1-diyl, and Y=O or S, in the racemic form, as well as the optical isomers (diastereomers and enantiomers) and the salts of the product of formula (I). The compounds of formula (I) are farnesyl transferase inhibitors which exhibit notable antitumor and antileukemic properties.
摘要翻译：式（I）的新型产物，其制备方法，含有它们的药物组合物及其在制备药物中的用途。在式（I）中，以下取代基是优选的：Ar表示取代或缩合的苯基或多环或杂环芳族基团，R表示通式为（CH 2）m -X1（CH 2）n Z的基团，其中X1 =单键，O，S; m = 0,1， n = 0,1,2; CH2基可以被取代; Z代表羧基，COOR6（R6 =烷基），CON（R7）（R8）（R7 =氢或烷基，R8 =氢，羟基，芳基磺酰基，杂环基，任选取代的氨基，任选取代的烷氧基或任选取代的烷基），PO OR 9）2（R 9 =氢或烷基），-NH-CO-T（T =氢或任选取代的烷基）基团，或不相关的，R 1和R 2 =氢或卤素或烷基，烷氧基，其被任选取代，烷硫基，烷氧基羰基或其它R1和R2在相邻的邻位形成含有1或2个杂原子的任选取代的杂环，R 3和R 4 =氢或卤素或烷基，烯基，烷氧基，烷硫基，羧基或烷氧基羰基，R5 =氢，烷基，烷硫基，X = O或S或-NH-，-CO-，亚甲基，乙烯基二烯基，烯-1,1-二基或环烷烃-1,1-二基，Y = O或S，外消旋形式，以及光学异构体（非对映异构体和对映体）和式（I）的产物的盐。式（I）化合物是具有显着的抗肿瘤和抗白血病性质的法呢基转移酶抑制剂。

44. 发明授权

US4271167A Hydroxyalkyl pyrid-2-yl dithiocarbamates, their preparation and their use 失效
标题翻译：羟基烷基吡啶-2-基二硫代氨基甲酸盐，其制备及其应用
公开(公告)号：US4271167A
公开(公告)日：1981-06-02
申请号：US094288
申请日：1979-11-14
申请人： Jean-Dominique Bourzat , Daniel Farge , Andre Leger , Gerard Ponsinet
发明人： Jean-Dominique Bourzat , Daniel Farge , Andre Leger , Gerard Ponsinet
IPC分类号： A61K31/44 , A61K31/4402 , A61P33/10 , C07D213/75 , C07D417/04 , C07D213/71
CPC分类号： C07D213/75
摘要： New dithiocarbamates of the formula: ##STR1## in which R.sub.1 is hydrogen or halogen in the 4-, 5- or 6-position, n is equal to 0 or 1, R.sub.2 represents hydrogen or various aliphatic or aromatic radicals which may be substituted, R.sub.3 represents hydrogen or various aliphatic radicals, and R.sub.4 represents a hydrogen atom or an alkyl radical, their optically active forms, and their salts, when such salts exist, are valuable anthelmintic agents. They may be made inter alia by reduction of the corresponding ketones.
摘要翻译：新的下式的二硫代氨基甲酸盐：其中R 1是氢或卤素在4-，5-或6-位，n等于0或1，其中R 2表示氢或各种脂族或芳族基团，其可以是 R 3代表氢或各种脂族基团，R 4表示氢原子或烷基，它们的旋光形式及其盐，当存在这些盐时，是有价值的驱虫剂。它们可以通过减少相应的酮而得到。

45. 发明授权

US06593482B2 Methods for preparing new taxoids and pharmaceutical compositions containing them 失效
标题翻译：制备新紫杉烷和含有它们的药物组合物的方法
公开(公告)号：US06593482B2
公开(公告)日：2003-07-15
申请号：US10029954
申请日：2001-12-31
申请人： Hervé Bouchard , Jean-Dominique Bourzat , Alain Commerçon , Iwao Ojima
发明人： Hervé Bouchard , Jean-Dominique Bourzat , Alain Commerçon , Iwao Ojima
IPC分类号： C07D30500
CPC分类号： C07D205/08 , C07D305/14
摘要： Methods of preparing methylthiomethyloxy taxoids of formula (XXXIV) from baccatin and &bgr;-lactam are presented. These new taxoids display noteworthy anti-tumor and anti-leukemic properties.
摘要翻译：提出了从浆果赤霉素和β-内酰胺制备式（XXXIV）的甲硫基甲氧基紫杉烷的方法。这些新型紫杉醇具有显着的抗肿瘤和抗白血病特性。

46. 发明授权

US06444825B1 Process for the preparation of an oxazolidinecarboxylic acid which is useful for preparing therapeutically active taxoids 失效
标题翻译：可用于制备治疗活性紫杉烷的恶唑烷羧酸的制备方法
公开(公告)号：US06444825B1
公开(公告)日：2002-09-03
申请号：US08564345
申请日：1995-12-14
申请人： Jean-Dominique Bourzat , Alain Commerçon
发明人： Jean-Dominique Bourzat , Alain Commerçon
IPC分类号： C07D26302
CPC分类号： C07D263/04 , C07D305/14
摘要： A method for preparing an oxazolidinecarboxylic acid of general formula (I), which is useful for preparing therapeutically active taxoids of general formula (III), from an oxazolidinecarboxylic acid of general formula (II). In formulae (I), (II) and (III), R is a hydrogen atom or an acetyl radical; R1 is a benzyl radical or a radical of the general formula R2—O—CO—, wherein R2 is an optionally substituted alkyl radical, alkenyl, alkynyl, cycloalkyl, cycloalkenyl, bicycloalkyl, phenyl or heterocyclyl; each of R3 and R4, which are the same or different, is hydrogen, alkyl, alkoxy, optionally substituted aryl or optionally substituted aralkyl, or together they form a 4-7 membered ring; R5 is alkenyl, alkynyl, phenyl, formyl, alkanoyl, aroyl, hydroxymethyl, carboxy or alkyloxycarbonyl; and R′ is a hydrogen atom or an alkali or alkaline-earth metal atom or an alkyl radical with 1-4 carbon atoms optionally substituted by phenyl radical.
摘要翻译：一种制备通式（I）的恶唑烷羧酸的方法，其可用于由通式（II）的恶唑烷羧酸制备通式（III）的治疗活性紫杉烷类。在式（I），（II）和（III）中，R是氢原子或乙酰基; R 1是苄基或通式R 2 -O-CO-的基团，其中R 2是任选取代的烷基，烯基，炔基，环烷基，环烯基，双环烷基，苯基或杂环基; R 3和R 4各自相同或不同，为氢，烷基，烷氧基，任选取代的芳基或任选取代的芳烷基，或一起形成4-7元环; R5是烯基，炔基，苯基，甲酰基，烷酰基，芳酰基，羟甲基，羧基或烷氧基羰基; 并且R'是氢原子或碱金属或碱土金属原子或任选被苯基取代的具有1-4个碳原子的烷基。

47. 发明授权

US5223529A N-phenylamides and medicinal products containing them 失效
标题翻译： N-苯甲酰胺和含有它们的药物
公开(公告)号：US5223529A
公开(公告)日：1993-06-29
申请号：US522137
申请日：1990-05-11
申请人： Jean-Dominique Bourzat , Marc Capet , Claude Cotrel , Claude Guyon , Gerard Roussel , Franco Manfre
发明人： Jean-Dominique Bourzat , Marc Capet , Claude Cotrel , Claude Guyon , Gerard Roussel , Franco Manfre
IPC分类号： C07D209/42 , A61K31/16 , A61K31/395 , A61K31/40 , A61K31/403 , A61K31/404 , A61K31/405 , A61K38/00 , A61P1/00 , A61P1/04 , A61P25/00 , A61P25/02 , A61P25/04 , A61P25/18 , A61P35/00 , C07C209/42 , C07C231/02 , C07C237/06 , C07C237/08 , C07C237/10 , C07C237/24 , C07C275/28 , C07C275/34 , C07C323/63 , C07D233/60 , C07D295/18 , C07K5/06
CPC分类号： C07K5/06052 , C07C209/42 , C07C237/24 , C07C275/28 , C07C275/34 , C07C323/63 , C07K5/06026 , A61K38/00
摘要： Compounds of formula: ##STR1## in which R.sub.1 is (a) a phenyl radical or a substituted phenyl radical, (b) a chain --CH(R.sub.8)--COOR.sub.4, (c) a chain --CH.sub.2 --CO--NR.sub.5 R.sub.6 or (d) a phenylalkyl radical, R.sub.2 is a methylene or ethylene radical or a radical --CH(R.sub.7)--, R.sub.3 is a 1- or 2-naphthyl radical, 2- or 3-indolyl or phenylamino radical in which the phenyl ring is optionally substituted on the understanding that, when R.sub.3 is 1- or 2-naphthyl or 2- or 3-indolyl radical, R.sub.7 cannot represent a benzyl, alkylthioalkyl or phenyl radical, as well as, when R.sub.2 is a radical --CH(R.sub.7)--, their racemates and their stereoisomers, and medicinal products containing them.
摘要翻译：其中R 1是（a）苯基或取代的苯基，（b）链-CH（R 8）-COOR 4，（c）链-CH 2 -CO-NR 5 R 6或（d ）苯基烷基，R 2是亚甲基或亚乙基或基团-CH（R 7） - ，R 3是1-或2-萘基，2-或3-吲哚基或苯基氨基，其中苯环被任选取代应理解的是，当R 3为1-或2-萘基或2-或3-吲哚基时，R 7不能表示苄基，烷硫基烷基或苯基，以及当R 2为基团-CH（R 7）其外消旋体及其立体异构体，以及含有它们的药用产品。

48. 发明授权

US5102890A Pyrrole derivatives, their preparation and pharmaceutical compositions which contain them 失效
标题翻译：吡咯衍生物，它们的制备和含有它们的药物组合物
公开(公告)号：US5102890A
公开(公告)日：1992-04-07
申请号：US402457
申请日：1989-09-05
申请人： Jean-Dominique Bourzat , Marc Capet , Claude Cotrel , Richard Labaudiniere , Philippe Pitchen , Gerard Roussel
发明人： Jean-Dominique Bourzat , Marc Capet , Claude Cotrel , Richard Labaudiniere , Philippe Pitchen , Gerard Roussel
IPC分类号： C07D471/04 , C07D519/00
CPC分类号： C07D471/04
摘要： This invention relates to pyrrole derivatives of formula: ##STR1## in which A forms with the pyrrole ring an isoindoline, 6,7-dihydro-5H-pyrrolo[3,4-b]pyrazine, 2,3,6,7-tetrahydro-5H-[1,4]oxathiino[2,3-c]pyrrole or 2,3,6,7-tetrahydro-5H-[1,4]dithiino[2,3-c]pyrrole ring-system and Hetis naphthyridinyl, pyridyl or quinolyl which is unsubstituted or substituted with halogen, (1 to 4 C) alkyl, (1 to 4 C) alkyloxy, (1 to 4 C) alkylthio or CF.sub.3 and R=(3 to 10 C) straight- or branched-chain alkenyl or alkyl which is unsubstituted or substituted with alkyloxy, alkylthio, (3 to 6 C) cycloalkyl, NH.sub.2, alkylamino, dialkylamino, alkylcarbonylamino, (in which the amino portion is optionally substituted with alkyl), 1- or 2-piperazinyl, piperidyl, piperidino, morpholino, pyrrolidinyl, 1-azetidinyl, carbamoyl, alkylcarbamoyl, dialkylcarbamoyl, (1-piperazinyl)carbonyl, piperidinocarbonyl, (1-pyrrolidinyl)carbonyl, phenyl, pyridyl, 1-imidazolyl, or alternatively R=2- or 3-pyrrolidinyl, 2-, 3- or 4-piperidyl, on the understanding that the alkyl radicals are straight- or branched-chain radicals and contain, except where specifically stated, 1 to 10 C, and that the piperazinyl, piperidino, piperidyl, pyrrolidinyl and azetidinyl radicals can be unsubstituted or substituted at any position with alkyl, alkylcarbonyl, benzyl or hydroxyalkyl, or can alternatively form a lactam group with the nitrogen atom of the ring, and, where they exist, their pharmaceutically acceptable salts and optical isomers, are useful as anxiolytics.
摘要翻译：本发明涉及下式的吡咯衍生物：其中A与吡咯环形成异吲哚啉，6,7-二氢-5H-吡咯并[3,4-b]吡嗪，2,3,6， -7- [1,4]恶二唑并[2,3-c]吡咯或2,3,6,7-四氢-5H- [1,4]二硫杂环[2,3-c]吡咯环体系和未取代的或被卤素取代的吡啶基或喹啉基，（1-4C）烷基，（1-4C）烷氧基，（1-4C）烷硫基或CF3和R =（3-10C）直链 - 或支链烯基或烷基，其未被取代或被烷氧基，烷硫基，（3至6 C）环烷基，NH 2，烷基氨基，二烷基氨基，烷基羰基氨基（其中氨基部分任选被烷基取代）取代， 2-哌嗪基，哌啶基，哌啶子基，吗啉代，吡咯烷基，1-氮杂环丁烷基，氨基甲酰基，烷基氨基甲酰基，二烷基氨基甲酰基，（1-哌嗪基）羰基，哌啶子基羰基，（1-吡咯烷基）羰基，苯基，吡啶基，1-咪唑基， 2-或3-吡咯烷基，2-，3-或4-哌啶基基于这样的理解，烷基是直链或支链基，并含有，除非特别说明为1-10个碳原子，并且哌嗪基，哌啶子基，哌啶基，吡咯烷基和氮杂环丁烷基可以是未取代的或任何取代的与烷基，烷基羰基，苄基或羟基烷基的位置，或者可选择地与环的氮原子形成内酰胺基，并且如果它们存在，其药学上可接受的盐和旋光异构体可用作抗焦虑剂。

49. 发明授权

US4994569A 5,6-dihydro-4H-1,3-oxa(or thia)zine derivatives, their preparation and compositions containing them 失效
标题翻译： 5,6-二氢-4H-1,3-氧杂吖嗪衍生物，它们的制备方法和含有它们的组合物
公开(公告)号：US4994569A
公开(公告)日：1991-02-19
申请号：US430127
申请日：1989-11-01
申请人： Jean-Dominique Bourzat , Claude Cotrel , Claude Guyon , Philippe Pitchen
发明人： Jean-Dominique Bourzat , Claude Cotrel , Claude Guyon , Philippe Pitchen
IPC分类号： A61K31/535 , A61K31/54 , A61P1/00 , A61P1/04 , A61P3/04 , A61P21/00 , A61P25/00 , A61P25/18 , C07D265/10 , C07D279/06 , C07D413/00 , C07D413/04 , C07D413/12 , C07D417/00 , C07D417/04
CPC分类号： C07D413/04 , C07D265/10 , C07D279/06 , C07D413/12 , C07D417/04
摘要： Compounds of formula: ##STR1## in which R.sub.1 denotes 2-indolyl, 2-thienyl, 3-furyl, naphthyl, phenyl, or phenyl substituted with one or two halogen atoms, with alkoxy, alkyl, nitro, acylamino, alkylthio, acyl, trifluoromethoxy, morpholino, piperidino, amino, mono- or dialkylamino or, at the 3- and 4-positions, with methylenedioxyR.sub.2 denotes phenyl or phenyl substituted with one or two halogen atoms, with one or two alkyl radicals, with alkoxy, nitro, trifluoromethyl or hydroxy or, at the 3- and 4-positions, with methylenedioxy andeither X denotes oxygen andR.sub.3 denotes phenyl R.sub.4, R.sub.5 and R.sub.6 denote hydrogen, orR.sub.3 and R.sub.4 denote hydrogen, R.sub.5 denotes hydrogen or methyl and R.sub.6 denotes phenyl or one of R.sub.3 and R.sub.4 denotes methyl and the other hydrogen, R.sub.5 denotes hydrogen and R.sub.6 denotes phenyl,or X denotes sulphur, R.sub.3 denotes phenyl and R.sub.4, R.sub.5 and R.sub.6 denote hydrogen; the said acyl, alkyl and alkoxy radicals and acyl, alkyl and alkoxy portions containing 1 to 4 carbon atoms each in a straight or branched chain; and their salts are useful in the treatment and prevention of disorders in which therapy with a cholecystokinin antagonist is indicated.
摘要翻译：其中R 1表示2-吲哚基，2-噻吩基，3-呋喃基，萘基，苯基或被一个或两个卤素原子取代的苯基与烷氧基，烷基，硝基，酰氨基，烷硫基，酰基，三氟甲氧基，吗啉代，哌啶子基，氨基，单或二烷基氨基，或在3-和4-位与亚甲二氧基R2表示苯基或被一个或两个卤素原子取代的苯基，一个或两个烷基与烷氧基，硝基，三氟甲基或羟基，或在3-和4-位与亚甲二氧基，X表示氧，R3表示苯基R4，R5和R6表示氢，或R3和R4表示氢，R5表示氢或甲基，R6表示表示苯基或R 3和R 3中的一个表示甲基，另一个氢，R 5表示氢，R 6表示苯基，或X表示硫，R 3表示苯基，R 4，R 5和R 6表示氢; 所述酰基，烷基和烷氧基以及在直链或支链中各自含有1至4个碳原子的酰基，烷基和烷氧基部分; 其盐可用于治疗和预防用缩胆囊素拮抗剂治疗的病症。

50. 发明授权

US4898871A Pyrrole derivatives and pharmaceutical compositions which contain them as hypnotics and anticonvulsants 失效
标题翻译：含有它们作为催眠剂和抗惊厥药的吡咯衍生物和药物组合物
公开(公告)号：US4898871A
公开(公告)日：1990-02-06
申请号：US126352
申请日：1987-11-30
申请人： Jean-Dominique Bourzat , Marc Capet , Claude Cotrel , Richard Labaudiniere , Philippe Pitchen , Gerard Roussel
发明人： Jean-Dominique Bourzat , Marc Capet , Claude Cotrel , Richard Labaudiniere , Philippe Pitchen , Gerard Roussel
IPC分类号： C07D209/46 , A61K31/435 , A61K31/44 , A61K31/4427 , A61K31/47 , A61K31/495 , A61P21/02 , A61P25/08 , A61P25/20 , C07D401/04 , C07D401/14 , C07D471/04 , C07D519/00
CPC分类号： C07D401/04 , C07D471/04
摘要： Pyrrole derivatives of formula ##STR1## in which A forms with the pyrrole ring an isoindoline, 6,7-dihydro-5H-pyrrolo-[3,4-b]pyrazine, 2,3,6,7-tetrahydro-5H-[1,4]-oxathiino-[2,3-c]pyrrole or 2,3,6,7-tetrahydro-5H-[1,4]dithiino-[2,3-c]pyrrole ring-system, Y+0, S or NH, Het=naphthyridinyl or quinolyl which are unsubstituted or substituted with halogen, (1 to 4 C) alkyl, (1 to 4 C) alkyloxy, (1 to 4 C) alkylthio, CN or CF.sub.3 and R=(3 to 10 C) alkenyl or alkyl which is unsubstituted or substituted with alkyloxy, alkylthio, cycloalkyl, alkylcarbonyl, cycloalkylcarbonyl or cycloalkylcarbamoyl in which the cycloalkyl portions contain 3 to 6 C, NH.sub.2, alkylamino, dialkylamino, alkylcarbonylamino, 1- or 2-piperazinyl, piperidyl, piperidino, morpholino, 1-azetidinyl, pyrrolidinyl, carbamoyl, alkylcarbamoyl, dialkylcarbamoyl, (1-piperazinyl)carbonyl, piperidinocarbonyl, piperidylcarbonyl, (1-pyrrolidinyl)carbonyl, morpholinocarbonyl, aminoalkylcarbamoyl, alkylaminoalkylcarbamoyl, dialkylaminoalkylcarbamoyl, alkyloxyalkylcarbamoyl, phenyl, pyridyl, or 1-imidazolyl, or R=2- or 3-pyrrolidinyl, or 1-imidazolyl, or 2-, 3- or 4-piperidyl, the aforesaid piperazinyl, piperidino, piperidyl, pyrrolidinyl, and azetidinyl radicals being unsubstituted or substituted at any position by alkyl, OH, alkylcarbonyl, benzyl, or hydroxyalkyl, or can form (i) a lactam group with the nitrogen atom of the ring or (ii) a 2-spirodioxolane residue with a carbon of the ring, and the said alkyl radicals containing 1 to 10 C except where specifically stated, are useful as anxiolytics.
摘要翻译：其中A与吡咯环形成异构吲哚，6,7-二氢-5H-吡咯并 - [3,4-b]吡嗪，2,3,6,7-四氢-5H- [ 1,4] - 氧硫杂环丁烷并[2,3-c]吡咯或2,3,6,7-四氢-5H- [1,4]二硫基 - [2,3-c]吡咯环系统，Y + （1-4C）烷基，（1-4C）烷氧基，（1-4C）烷硫基，CN或CF3和R =（3）中的任意一个或多个取代或未取代或被卤素取代的苯甲酰基，未取代或被烷氧基，烷硫基，环烷基，烷基羰基，环烷基羰基或环烷基氨基甲酰基取代的烯基或烷基，其中环烷基部分含有3至6个C，NH 2，烷基氨基，二烷基氨基，烷基羰基氨基，1-或2-哌嗪基，哌啶基羰基，（1-吡咯烷基）羰基，吗啉代羰基，氨基烷基氨基甲酰基，烷基氨基烷基氨基甲酰基，二烷基氨基烷基氨基酰基，烷氧基烷基氨基甲酰基，苯基，吡啶基或1-咪唑基，或R = 2-或3-吡咯烷基或1-咪唑基，或2-，3-或4-哌啶基，上述哌嗪基，哌啶子基，哌啶基，吡咯烷基和氮杂环丁烷基是未取代的或在任何位置被烷基，OH，烷基羰基，苄基或羟基烷基取代，或可以形成（i）具有环的氮原子的内酰胺基团或（ii）2-螺环和所述含有1至10个C的烷基，除非特别说明，可用作抗焦虑剂。

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