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    Intermediates in a resolution process for racemic spiro hydantoins
    1.
    发明授权
    Intermediates in a resolution process for racemic spiro hydantoins 失效
    中间体在外消旋螺乙素的解决过程中

    公开(公告)号：US5006657A

    公开(公告)日：1991-04-09

    申请号：US543986

    申请日：1990-06-25

    申请人： Marcus Brackeen ,  Harry R. Howard, Jr.

    发明人： Marcus Brackeen ,  Harry R. Howard, Jr.

    IPC分类号： C07D471/10 ,  C07D491/10

    CPC分类号： C07D471/10 ,  C07D491/10

    摘要： A novel three-step process for resolving a racemic spiro-hydantoin compound into its optical antipodes is disclosed, which involves (1) reacting said racemic compound with an optically-active asymmetric isocyanate of the formula RNCO, wherein R is (S)- or (R)-1-phenylethyl or (S)-or (R)-1-(1-naphthyl)ethyl, to form the corresponding diastereomeric ureido compound; (2) separating the resulting diastereomeric mixture into its component parts, and (3) thereafter converting the separated ureido diasteromers obtained in step (b) to the corresponding asymmetric hydantoin compounds by treatment with an alkali metal lower alkoxide (C.sub.1 -C.sub.4), followed by acidification, whereupon the desired optical isomer is obtained. The final products so obtained, such as (4S)-(+)-6-fluoro-2,3-dihydro-spiro-[4H-1-benzopyran-4,4'-imidazolidine]-2',5'-dione(sorbinil) and (5'S)-3'-chloro-5', 6',7',8'-tetrahydro-spiro[imidazolidine-4,5'-quinoline]-2,5-dione, are known to be useful in preventing or alleviating certain chronic diabetic complications. The aforementioned diastereomeric ureido intermediates are novel compounds.

    摘要翻译： 公开了一种用于将外消旋螺 - 乙内酰脲化合物分解成其光学对映体的新型三步法，其包括（1）使所述外消旋化合物与式RNCO的光学活性不对称异氰酸酯反应，其中R是（S） - 或 （R）-1-苯乙基或（S） - 或（R）-1-（1-萘基）乙基，形成相应的非对映异构脲基化合物; （2）将得到的非对映异构体混合物分离成其组分，（3）此后通过用碱金属低级醇盐（C1-C4）处理将步骤（b）中得到的分离的脲基非对映异构体转化成相应的不对称乙内酰脲化合物，随后 通过酸化，得到所需的旋光异构体。 得到的最终产物如（4S） - （+） - 6-氟-2,3-二氢 - 螺 - [4H-1-苯并吡喃-4,4'-咪唑烷e] -2' 二酮（sorbinil）和（5'S）-3'-氯-5'，6'，7'，8'-四氢 - 螺[咪唑烷-4,5'-喹啉] -2,5-二酮已知为 可用于预防或减轻某些慢性糖尿病并发症。 上述非对映异构体脲基中间体是新化合物。

    Novel resolution process for racemic spiro-hydantoins
    2.
    发明授权
    Novel resolution process for racemic spiro-hydantoins 失效
    外消旋螺 - 乙内酰脲的新颖解决方法

    公开(公告)号：US4952694A

    公开(公告)日：1990-08-28

    申请号：US224966

    申请日：1988-07-27

    申请人： Marcus Brackeen ,  Harry R. Howard, Jr.

    发明人： Marcus Brackeen ,  Harry R. Howard, Jr.

    IPC分类号： A61K31/35 ,  A61K31/38 ,  A61K31/415 ,  A61K31/4184 ,  A61K31/4188 ,  A61P3/10 ,  C07D233/72 ,  C07D235/02 ,  C07D471/10 ,  C07D471/20 ,  C07D491/10 ,  C07D491/107 ,  C07D491/20 ,  C07D495/10 ,  C07D495/20

    CPC分类号： C07D471/10 ,  C07D491/10

    摘要： A novel three-step process for resolving a racemic spiro-hydantoin compound into its optical antipodes is disclosed, which involves (1) reacting said racemic compound with an optically-active asymmetric isocyanate of the formula RNCO, wherein R is (S)- or (R)-1-phenylethyl or (S) or (R)-1-(1-naphthyl)ethyl, to form the corresponding diastereomeric uredio compound; (2) separating the resulting diastereomeric mixture into its component parts, and (3) thereafter converting the separated ureido diastereomers obtained in step (b) to the corresponding asymmetric hydantoin compounds by treatment with an alkali metal lower alkoxide (C.sub.1 -C.sub.4), followed by acidification, whereupon the desired optical isomer is obtained. The final products so obtained, such as (4S)-(+)-6-fluoro-2,3-dihydro-spiro[4H-1-benzopyran-4,4'-imidazolidine]-2', 5'-dione (sorbinil) and (5'S)-3'-chloro-5', 6', 7', 8'-tetra-hydro-spiro[imidazolidine-4,5'-quinoline]-2,5-dione, are known to be useful in preventing or alleviating certain chronic diabetic complications. The aforementioned diastereomeric uredio intermediates are novel compounds.

    Method of treating anxiety and depression with 1-phenyl-2(1H,3H)-indolone psycho-therapeutic agents
    9.
    发明授权
    Method of treating anxiety and depression with 1-phenyl-2(1H,3H)-indolone psycho-therapeutic agents 失效
    用1-苯基-2（1H，3H） - 吲哚酮心理治疗剂治疗焦虑和抑郁症的方法

    公开(公告)号：US4977178A

    公开(公告)日：1990-12-11

    申请号：US382614

    申请日：1989-07-19

    申请人： Harry R. Howard, Jr. ,  Reinhard Sarges

    发明人： Harry R. Howard, Jr. ,  Reinhard Sarges

    IPC分类号： C07C43/225 ,  C07D209/08 ,  C07D209/34 ,  C07D209/38

    CPC分类号： C07D209/08 ,  C07C43/225 ,  C07D209/34 ,  C07D209/38

    摘要： Certain substituted 1-phenyl-3-(aminoalkylidene)-2(1H,3H)-indolones are highly potent gabaergic agents, valuable in the treatment of individuals suffering from schizophrenia or reversing the side effects of a previously or concurrently administered neuroleptic agent; or in the treatment of epilepsy. A wider class of substituted 1-phenyl-3-(aminoalkylidene)-2(1H,3H)-indolones, together with 1-phenyl-3-(2-pyrrolidinylidene)-2(1H,3H)-indolones, and homologs thereof, are valuable in the treatment of anxiety.

    摘要翻译： 某些取代的1-苯基-3-（氨基亚烷基）-2（1H，3H） - 吲哚酮是非常有效的gabaergic试剂，在治疗患有精神分裂症或逆转先前或同时施用的精神抑制剂的副作用的个体中是有价值的; 或治疗癫痫。 更广泛类别的取代的1-苯基-3-（氨基亚烷基）-2（1H，3H） - 吲哚酮与1-苯基-3-（2-吡咯烷亚基）-2（1H，3H） - 吲哚酮及其同系物 ，在治疗焦虑方面是有价值的。

    Indolinone derivatives
    10.
    发明授权
    Indolinone derivatives 失效
    吲哚啉酮衍生物

    公开(公告)号：US4960785A

    公开(公告)日：1990-10-02

    申请号：US346115

    申请日：1988-12-16

    申请人： Harry R. Howard, Jr. ,  Reinhard Sarges

    发明人： Harry R. Howard, Jr. ,  Reinhard Sarges

    IPC分类号： C07D209/34 ,  C07D209/96 ,  C07D491/056

    CPC分类号： C07D209/34 ,  C07D209/96 ,  Y10S514/866

    摘要： A series of novel 3-mono(substituted methyl)- and 3,3-di(substituted methyl)-2-oxo-indoline-1-alkanoic acid compounds have been prepared, including their lower alkyl esters and unsubstituted amide derivatives, as well as the base salts of said acids with pharmacologically acceptable cations. These compounds are useful in therapy as aldose reductase inhibitors for the control of certain chronic diabetic complications. Said oxindole-1-alkanoic acid compounds are of the formulae: ##STR1## wherein X is hydrogen and X.sup.1 is hydrogen, hydroxy, fluorine, chlorine, bromine, C.sub.1 -C.sub.4 alkyl or C.sub.1 -C.sub.4 alkoxy; or X and X.sup.1, when taken separately, are each chlorine, C.sub.1 -C.sub.4 alkyl or C.sub.1 -C.sub.4 alkoxy, and when taken together are --OCH.sub.2 (CH.sub.2).sub.n O-- at the 4,5-, 5,6- or 6,7-positions of the molecule wherein n is zero or one; R.sub.1 is hydrogen or methyl; R.sub.2 is hydrogen, C.sub.1 -C.sub.4 alkyl or phenylalkyl having up to three carbon atoms in the alkyl moiety wherein said phenylalkyl is optionally substituted with up to two chlorine substituents on the phenyl ring; R.sub.3 is naphthylmethyl, furfuryl, thenyl, benzothienylmethyl, benzoxazolylmethyl, benzothiazolylmethyl or phenylalkyl having up to three carbon atoms in the alkyl moiety wherein said phenylalkyl is optionally substituted with up to two identical or non-identical substituents on the phenyl ring, said identical substituents being fluorine, chlorine, bromine, trifluoromethyl, C.sub.1 -C.sub.4 alkyl or C.sub.1 -C.sub.4 alkoxy and said non-identical substituents being chlorine, methyl, methoxy or trifluoromethyl; and Y is hydrogen, fluorine, chlorine, C.sub.1 -C.sub.4 alkyl or C.sub.1 -C.sub.4 -alkoxy.

    摘要翻译： PCT No.PCT / US86 / 01429 Sec。 371日期：1988年12月16日 102（e）1988年12月16日PCT PCT 1986年6月10日。一系列新型3-单（取代甲基） - 和3,3-二（取代甲基）-2-氧代 - 二氢吲哚-1-链烷酸 已经制备了酸化合物，包括其低级烷基酯和未取代的酰胺衍生物，以及所述酸与药理学上可接受的阳离子的碱式盐。 这些化合物可用于治疗某些慢性糖尿病并发症的醛糖还原酶抑制剂。 所述羟吲哚-1-链烷酸化合物具有下式：其中X是氢，X 1是氢，羟基，氟，氯，溴，C 1 -C 4烷基或C 1 -C 4烷氧基; 或X和X 1分别为氯，C 1 -C 4烷基或C 1 -C 4烷氧基，并且当在4,5-，5,6-或6,7时共同为-OCH 2（CH 2）n O- 分子的位置，其中n为0或1; R1是氢或甲基; R2是氢，C1-C4烷基或在烷基部分具有至多三个碳原子的苯基烷基，其中所述苯基烷基任选被苯环上最多两个氯取代基取代; R3是在烷基部分中具有至多三个碳原子的萘甲基，糠基，噻吩基，苯并噻吩基甲基，苯并恶唑基甲基，苯并噻唑基甲基或苯基烷基，其中所述苯基烷基任选被苯环上最多两个相同或不相同的取代基取代，所述相同的取代基是 氟，氯，溴，三氟甲基，C 1 -C 4烷基或C 1 -C 4烷氧基，所述不相同的取代基是氯，甲基，甲氧基或三氟甲基; Y是氢，氟，氯，C1-C4烷基或C1-C4-烷氧基。