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71. 发明授权

US4876345A Indene compounds 失效
标题翻译：茚化合物
公开(公告)号：US4876345A
公开(公告)日：1989-10-24
申请号：US202597
申请日：1988-06-06
申请人： Shozo Nakaoku , Kazuhiko Sakuma , Yasuhiro Oshika , Kazuo Ohira
发明人： Shozo Nakaoku , Kazuhiko Sakuma , Yasuhiro Oshika , Kazuo Ohira
IPC分类号： A61K31/495 , A61K31/443 , A61K31/445 , A61K31/55 , A61P3/00 , A61P9/08 , A61P9/10 , C07C67/00 , C07C213/00 , C07C217/74 , C07D243/00 , C07D295/08 , C07D295/096 , C07D317/00 , C07D317/70 , C07D405/04 , C07D407/12 , C07D417/12
CPC分类号： C07D295/096 , C07D317/70 , C07D407/12 , C07D417/12
摘要： The invention provides an indene compound represented by the following general formula (I): ##STR1## wherein R.sub.1 means a lower alkyl group, R.sub.2 and R.sub.3 denote a lower alkyl group individually or an alkylenedioxy group in combination, and R.sub.4 and R.sub.5 mean individually a substituted or unsubstituted lower alkyl or aryl group or in combination a substituted or unsubstituted piperidino, piperazinyl or homopiperazinyl group together with the adjacent nitrogen atom, with a proviso that not both R.sub.4 and R.sub.5 are a methyl group at the same time.

72. 发明授权

US4873243A Derivatives of 3-imino-pyridazine, process for obtaining them and pharmaceutical compositions containing them 失效
标题翻译： 3-亚氨基 - 哒嗪的衍生物，获得它们的方法和含有它们的药物组合物
公开(公告)号：US4873243A
公开(公告)日：1989-10-10
申请号：US923901
申请日：1986-10-28
申请人： Camille G. Wermuth , Gilbert Schlewer , Michel Heaulme
发明人： Camille G. Wermuth , Gilbert Schlewer , Michel Heaulme
IPC分类号： A01N43/58 , A61K31/50 , A61P25/20 , A61P25/24 , A61P25/26 , C07D237/00 , C07D317/00 , C07D333/00 , C07D413/06 , C07D413/14 , C07D417/06
CPC分类号： C07D413/06 , C07D413/14 , C07D417/06
摘要： The invention relates to derivatives of 2,3-dihydro 3-imino-pyridazine responding to general formula: ##STR1## in which: A represents an atom of oxygen or of sulfur;R.sub.1 represents a lower alkyl group, or an aromatic group selected from:the phenyl group;the phenyl groups mono- or poly-substituted by a halogen group, a lower alkyl group, a lower alkoxy group, a nitro group, a hydroxy or methylenedioxy group;the naphthyl group;the furyl group;the thienyl group or the pyridyl group;R.sub.2 and R.sub.3 each designate independently hydrogen or a lower alkyl group; a phenyl group, or R.sub.2 and R.sub.3, taken together, constitute, with the 2 atoms of the pyridazinic cycle to which they are bonded, a benzene ring, and their pharmaceutically acceptable salts. Application: antidepressants or psychotonics.
摘要翻译：本发明涉及响应以下通式的2,3-二氢-3-亚氨基 - 哒嗪衍生物：其中：A表示氧原子或硫原子; R1表示低级烷基或选自：苯基的芳基; 被卤素基，低级烷基，低级烷氧基，硝基，羟基或亚甲二氧基单取代或多取代的苯基; 萘基; 呋喃基; 噻吩基或吡啶基; R2和R3各自独立地表示氢或低级烷基; 苯基或R 2和R 3一起构成与其键合的哒嗪基的2个原子，苯环及其药学上可接受的盐。应用：抗抑郁药或心理学。

73. 发明授权

US4859670A 2-Azolylmethyl-2-aryl-1,3-dioxolanes and the salts thereof, agents containing same, and the use thereof 失效
标题翻译： 2-唑基甲基-2-芳基-1,3-二氧戊环及其盐，含有它们的试剂及其用途
公开(公告)号：US4859670A
公开(公告)日：1989-08-22
申请号：US028193
申请日：1987-03-19
申请人： Klaus-Dieter Kampe , Wolfgang Raether , Walter Dittmar , Heinz Hanel
发明人： Klaus-Dieter Kampe , Wolfgang Raether , Walter Dittmar , Heinz Hanel
IPC分类号： A61K31/44 , A01N43/60 , A01N43/653 , A61K31/443 , A61K31/47 , A61P31/04 , C07D239/26 , C07D239/28 , C07D239/34 , C07D239/36 , C07D317/00 , C07D405/12 , C07D521/00
CPC分类号： C07D239/26 , A01N43/60 , A01N43/653 , C07D231/12 , C07D233/56 , C07D239/28 , C07D239/34 , C07D239/36 , C07D249/08
摘要： Compounds of the formula I ##STR1## in which A equals CH or N, Ar equals phenyl, naphthyl or thienyl, R.sup.1 equals alkyl or halogen, and Y is a number of nitrogen-containing heterocyclic rings, have an excellent antimycotic action.The compounds IIIa ##STR2## are valuable intermediates for the preparation thereof.
摘要翻译：其中A等于CH或N，Ar等于苯基，萘基或噻吩基，R1等于烷基或卤素，Y是多个含氮杂环的式I 的化合物具有优异的抗真菌作用。化合物IIIa IIIa是制备它们的有价值的中间体。

74. 发明授权

US4824970A Intermediates for the synthesis of carboxylic acids 失效
标题翻译：用于合成羧酸的中间体
公开(公告)号：US4824970A
公开(公告)日：1989-04-25
申请号：US891348
申请日：1986-07-31
申请人： Graziano Castaldi , Claudio Giordano
发明人： Graziano Castaldi , Claudio Giordano
IPC分类号： C07C51/00 , C07C57/30 , C07C67/00 , C07D317/34 , C07D317/00
CPC分类号： C07D317/34 , C07C51/00
摘要： Compounds are described of formula ##STR1## in which: Ar represents a aryl, possibly substituted;R represents a C.sub.1 -C.sub.4 alkyl;R' represents a hydroxyl, an alkoxy, an amino group possibly mono or di-alkyl substituted, or an O-M+ group where M+ represents the cation of an alkaline metal;X represents a hydrogen, chlorine, bromine or iodine atom, a hydroxyl, or an acyloxy, alkylsulphonyloxy or arylsulphonyloxy group.The compounds of formula I can be easily transformed into alphaarylalkanoic acids of formula ##STR2## in which Ar and R have the aforesaid meanings.
摘要翻译：化合物描述为式（I），其中：Ar表示可能被取代的芳基; R代表C1-C4烷基; R'表示羟基，烷氧基，可能单或二烷基取代的氨基，或者M +表示碱金属阳离子的O-M +基团; X表示氢，氯，溴或碘原子，羟基或酰氧基，烷基磺酰氧基或芳基磺酰氧基。式I化合物可以容易地转化成其中Ar和R具有上述含义的式（III）的α-芳基链烷酸。

75. 发明授权

US4824846A 2-Azolylmethyl-2-aryl-1,3-dioxolanes and the salts thereof, agents containing same, and the use thereof 失效
标题翻译： 2-唑基甲基-2-芳基-1,3-二氧戊环及其盐，含有它们的试剂及其用途
公开(公告)号：US4824846A
公开(公告)日：1989-04-25
申请号：US28087
申请日：1987-03-19
申请人： Klaus D. Kampe , Wolfgang Raether , Walter Dittmar , Heinz Hanel
发明人： Klaus D. Kampe , Wolfgang Raether , Walter Dittmar , Heinz Hanel
IPC分类号： C07D247/00 , A01N43/60 , A01N43/653 , A61K31/44 , A61K31/443 , A61K31/47 , A61P25/08 , C07D213/72 , C07D213/85 , C07D215/54 , C07D237/34 , C07D239/14 , C07D239/42 , C07D317/00 , C07D333/00 , C07D405/14 , C07D521/00 , A61K31/505
CPC分类号： C07D239/42 , A01N43/60 , A01N43/653 , C07D213/72 , C07D213/85 , C07D215/54 , C07D231/12 , C07D233/56 , C07D237/34 , C07D239/14 , C07D249/08
摘要： Compounds I ##STR1## where A equals CH or N; Ar equals naphthyl, thienyl or phenyl; R.sup.1 equals alkyl, F or Cl; g equals zero, 1 or 2; and Y equals various heterocyclic bases, and the acid-addition salts thereof, are described.Several preparation processes are described.The compounds IIIa ##STR2## where R.sup.1, g and Y are as specified in the case of the formula I, serve as intermediates for the preparation of these compounds. Processes are also specified for the preparation of IIIa.I represent valuable antimycotics.
摘要翻译：化合物I 其中A等于CH或N; Ar等于萘基，噻吩基或苯基; R1等于烷基，F或Cl; g等于零，1或2; 和Y等于各种杂环碱，并描述其酸加成盐。描述几个准备过程。其中R1，g和Y如式I所示的化合物IIIa用作制备这些化合物的中间体。还规定了制备IIIa的方法。我代表有价值的抗菌药。

76. 发明授权

US4762927A Indene compounds 失效
标题翻译：茚化合物
公开(公告)号：US4762927A
公开(公告)日：1988-08-09
申请号：US884649
申请日：1986-07-11
申请人： Shozo Nakaoku , Kazuhiko Sakuma , Yasuhiro Oshika , Kazuo Ohira
发明人： Shozo Nakaoku , Kazuhiko Sakuma , Yasuhiro Oshika , Kazuo Ohira
IPC分类号： A61K31/495 , A61K31/443 , A61K31/445 , A61K31/55 , A61P3/00 , A61P9/08 , A61P9/10 , C07C67/00 , C07C213/00 , C07C217/74 , C07D243/00 , C07D295/08 , C07D295/096 , C07D317/00 , C07D317/70 , C07D405/04 , C07D407/12 , C07D417/12
CPC分类号： C07D295/096 , C07D317/70 , C07D407/12 , C07D417/12
摘要： The invention provides an indene compound represented by the following general formula (I): ##STR1## wherein R.sub.1 means a lower alkyl group, R.sub.2 and R.sub.3 denote a lower alkyl group individually or an alkylenedioxy group in combination, and R.sub.4 and R.sub.5 mean individually a substituted or unsubstituted lower alkyl or aryl group or in combination a substituted or unsubstituted piperidino, piperazinyl or homopiperazinyl group together with the adjacent nitrogen atom, with a proviso that not both R.sub.4 and R.sub.5 are a methyl group at the same time.
摘要翻译：本发明提供由以下通式（I）表示的茚化合物：其中R 1表示低级烷基，R 2和R 3分别表示低级烷基或亚烷基二氧基，R 4和R 5 意指单独取代或未取代的低级烷基或芳基，或者组合取代或未取代的哌啶子基，哌嗪基或高哌嗪基与相邻的氮原子，条件是不同时R4和R5都是甲基。

77. 发明授权

US4739082A Enantiomerically pure mono acetal-protected diols, their preparation and use 失效
标题翻译：对映体纯的单缩醛保护的二醇，其制备和用途
公开(公告)号：US4739082A
公开(公告)日：1988-04-19
申请号：US717383
申请日：1985-03-29
申请人： Christian R. Noe , Max Knollmuller
发明人： Christian R. Noe , Max Knollmuller
IPC分类号： A01N43/30 , A01N43/90 , C07D307/93 , C07D317/00 , C07D407/12 , C07D493/08 , C07D311/00 , C07D311/78
CPC分类号： C07D307/93 , C07D407/12 , C07D493/08
摘要： Enantiomerically pure mono acetal-protected diols of the formula ##STR1## wherein A, B, C and D are hydrogen or a methyl group in any combination, M and N are aliphatic or araliphatic hydrocarbons, m and n are the numbers 0, 1 or 2, whereby the total of m plus n must be the number 1 or 2, their preparation and use for the syntheses of the pheromones (1R-exo)-Brevicomin, (1S-exo)-Brevicomin, (1R-endo)-Brevicomin and (1S-endo)-Brevicomin.
摘要翻译：对映体纯的单缩醛保护的式Ⅰ的二醇，其中A，B，C和D是氢或任何组合的甲基，M和N是脂族或芳脂族烃，m和n是数字0,1 （1R-exo）-Brevicomin，（1S-exo）-Brevicomin，（1R-endo） - 的合成的制备和用途，其中m + n的总和必须为数字1或2， Brevicomin和（1S-endo）-Brevicomin。

78. 发明授权

US4739050A 2-phenyl-1,4-benzothiazin-3-one derivatives 失效
公开(公告)号：US4739050A
公开(公告)日：1988-04-19
申请号：US928277
申请日：1986-11-04
申请人： Iwao Jun-ichi , Iso Tadashi , Oya Masayuki
发明人： Iwao Jun-ichi , Iso Tadashi , Oya Masayuki
IPC分类号： A61K31/54 , A61K31/5415 , A61P3/00 , A61P3/14 , A61P7/02 , A61P9/08 , A61P9/10 , A61P9/12 , C07D279/16 , C07D317/00 , C07D417/06 , C07D417/12 , C07D279/10 , A61K31/38
CPC分类号： C07D417/06 , C07D279/16 , C07D417/12
摘要： This invention relates to 2-arylbenzothiazine derivatives of the formula[I] and salts thereof, process of preparation and therapeutic drug comprising them for circulatory diseases, ##STR1## wherein R.sup.1 and R.sup.2 are the same or different and are hydrogen, lower alkyl, hydroxy, lower alkoxy, acyloxy, tetrahydropyranyloxy, halogen, nitro, amino, lower alkylamino or ##STR2## and the lower alkoxy group may be substituted by halogen, formyl, lower alkoxy or epoxy;R.sup.3 is hydrogen or lower alkyl;R.sup.4 is hydrogen, lower alkyl, cycloalkyl, hydroxy, lower alkoxy, mercapto, lower alkylthio, arylthio, halogen, cyano, formyl-lower alkyl, lower alkoxy-lower alkyl or ##STR3## R.sup.5,R.sup.6,R.sup.7 and R.sup.8 are the same or different and are hydrogen, lower alkyl, cycloalkyl, acyl, phenyl, pyridyl or substituted lower alkyl, and the phenyl or pyridyl group may be substituted by lower alkyl, hydroxy, lower alkoxy, lower alkylenedioxy, halogen, nitro, cyano, lower alkanoyloxy or halogeno-lower alkyl, and the substituent(s) of the substituted lower alkyl is(are) hydroxy, phenyl, phenyloxy, phenylcarbonyl or pyridyl, and such phenyl ring of the phenyl, phenyloxy or phenylcarbonyl group and the pyridyl group may further be resubstituted by lower alkyl, hydroxy, lower alkoxy, lower alkylenedioxy, halogen, nitro, cyano, lower alkanoyloxy or halogeno lower alkyl;R.sup.5 and R.sup.6, and R.sup.7 and R.sup.8 may join to form piperidine, piperazine or morpholine ring, and the piperidine or piperazine ring may be substituted by lower alkyl, phenyl, hydroxy-lower alkyl, phenyl-lower alkyl, phenylcarbonyl, phenylcarbonyl-lower alkyl, spheny-(hydroxy) lower alkyl, phenyl-lower alkenylcarbonyl or naphthoxy-(hydroxy)lower alkyl, and such phenyl ring of the phenyl, phenyl-lower alkyl, phenylcarbonyl, phenylcarbonyl-lower alkyl, phenyl-(hydroxy)lower alkyl or phenyl-lower alkenylcarbonyl group may further be resubstituted by lower alkyl, lower alkoxy, alkylenedioxy or halogen;Z is hydrogen, lower alkyl, lower alkoxy, hydroxy, halogen, cyano, nitro, halogeno-lower alkyl or lower alkanoyloxy;A is straight or branched lower alkylene;B is straight or branched lower alkylene which may be substituted by hydroxy; andn is 0 or 1, and when n is 0, both R.sup.4 and Z are not represent hydrogen atom at the same time.

79. 发明授权

US4732985A 2-oxygen containing heteroalkoxyalkyl dihydropyridine intermediates 失效
标题翻译：含2-氧的杂烷氧基烷基二氢吡啶中间体
公开(公告)号：US4732985A
公开(公告)日：1988-03-22
申请号：US927881
申请日：1986-11-05
申请人： David Alker , Simon F. Campbell , Peter E. Cross
发明人： David Alker , Simon F. Campbell , Peter E. Cross
IPC分类号： C07D317/00 , A61K31/4427 , A61K31/443 , A61K31/455 , A61K31/505 , A61P9/08 , A61P9/12 , C07D211/90 , C07D317/22 , C07D401/12 , C07D405/12 , C07D521/00 , C07D403/12
CPC分类号： C07D231/12 , C07D211/90 , C07D233/56 , C07D249/08 , C07D401/12 , C07D405/12
摘要： 1,4-Dihydropyridine anti-ischaemic and antihypertensive agent of the formula: ##STR1## or a pharmaceutically acceptable salt thereof, wherein R is 2-chlorophenyl, 2,3-dichlorophenyl or 2-chloro-3-trifluoromethylphenyl;R.sup.1 and R.sup.2 are each independently C.sub.1 -C.sub.4 alkyl;X is O or S;R.sup.3 is H or C.sub.1 -C.sub.4 alkyl; andR.sup.4 is 1,2,4-triazol-1-ylmethyl, imidazol-1-ylmethyl, azidomethyl, 2,4,5-trimethylimidazol-1-ylmethyl, 3,4-dihydro-4-oxopyrimidin-2-ylthiomethyl, pyrimidin-2-ylthiomethyl; pyrimidin-2-ylaminomethyl, 3,4-dihydro-4-oxopyrimidin-2-ylaminomethyl, 2-aminopyrimidin-4-yloxymethyl, methoxymethyl, 2-furyl, 2-pyridylmethyl, imidazol-2-yl, hydroxymethyl, aminomethyl, 1,2,4-triazol-4-ylmethyl or 2-hydroxyethyl, and intermediates leading thereto.
摘要翻译： 1,4-二氢吡啶抗缺血和抗高血压药剂，其分子式如下：其中R是2-氯苯基，2,3-二氯苯基或2-氯-3-三氟甲基苯基;或其药学上可接受的盐。 R1和R2各自独立地为C1-C4烷基; X是O或S; R3是H或C1-C4烷基; 并且R 4是1,2,4-三唑-1-基甲基，咪唑-1-基甲基，叠氮基甲基，2,4,5-三甲基咪唑-1-基甲基，3,4-二氢-4-氧代嘧啶-2-基硫甲基，嘧啶 -2-基硫甲基; 嘧啶-2-基氨基甲基，3,4-二氢-4-氧代嘧啶-2-基氨基甲基，2-氨基嘧啶-4-基氧基甲基，甲氧基甲基，2-呋喃基，2-吡啶基甲基，咪唑-2-基，羟甲基，氨基甲基， 2,4-三唑-4-基甲基或2-羟乙基，以及通向其的中间体。

80. 发明授权

US4721723A Anti-depressant crystalline paroxetine hydrochloride hemihydrate 失效
标题翻译：抗抑郁结晶帕罗西汀盐酸盐半水合物
公开(公告)号：US4721723A
公开(公告)日：1988-01-26
申请号：US922530
申请日：1986-10-23
申请人： Roger D. Barnes , Marian W. Wood-Kaczmar , Alan D. Curzons , Ian R. Lynch , John E. Richardson , Philip C. Buxton
发明人： Roger D. Barnes , Marian W. Wood-Kaczmar , Alan D. Curzons , Ian R. Lynch , John E. Richardson , Philip C. Buxton
IPC分类号： C07D317/00 , A61K31/443 , A61K31/445 , A61K31/451 , A61P25/24 , A61P25/26 , A61P43/00 , C07D211/22 , C07D405/12
CPC分类号： C07D405/12 , C07D211/22
摘要： The invention provides crystalline paroxetine hydrochloride hemihydrate, processes for its preparation, compositions containing the same and its therapeutic use as an anti-depressant.
摘要翻译：本发明提供了结晶帕洛西汀盐酸盐半水合物，其制备方法，含有该组合物的组合物及其作为抗抑郁剂的治疗用途。

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