Process for the preparation of 1,1'-methane-bis (Hydantoin)
    33.
    发明授权
    Process for the preparation of 1,1'-methane-bis (Hydantoin) 失效
    制备1,1'-甲烷 - 双(乙内酰脲)的方法

    公开(公告)号:US5554762A

    公开(公告)日:1996-09-10

    申请号:US442231

    申请日:1995-05-15

    CPC分类号: C07D233/74 C07F9/3813

    摘要: This invention relates to method for the preparation of 1,1'-methane-bis(hydantoin). 1,1'-methane-bis(hydantoin) is an intermediate in the preparation of N-(phosphonomethyl)glycine which is a well known herbicide and plant growth regulator.

    摘要翻译: 本发明涉及制备1,1'-甲烷 - 双(乙内酰脲)的方法。 1,1'-甲烷 - 双(乙内酰脲)是制备N-(膦酰基甲基)甘氨酸的中间体,其是公知的除草剂和植物生长调节剂。

    1,3-Dihydro-2H-imidazo[4,5-B]quinolin-2-one derivatives
    34.
    发明授权
    1,3-Dihydro-2H-imidazo[4,5-B]quinolin-2-one derivatives 失效
    1,3-二氢-2H-咪唑并[4,5-B]喹啉-2-酮衍生物

    公开(公告)号:US5521187A

    公开(公告)日:1996-05-28

    申请号:US204412

    申请日:1994-03-15

    摘要: Novel 1,3-dihydro-2H-imidazo[4,5-b]quinolin-2-one derivatives of formula ##STR1## wherein R is hydrogen, C.sub.1-6 alkyl, C.sub.3-6 cycloalkyl, phenyl optionally substituted with from 1 to 3 substituents each independently selected from halo, hydroxy, C.sub.1-6 alkyloxy, C.sub.5-6 cycloalkyloxy, C.sub.1-6 alkyl or trifluoromethyl; pyridinyl; thienyl optionally substituted with halo or C.sub.1-6 alkyl; and>C.dbd.X is a radical of formula>C.dbd.O (a),>C.dbd.N--O--R.sup.1 (b),or>C.dbd.CH--R.sup.2 (c);the pharmaceutically acceptable addition salts and stereochemically isomeric forms thereof, said compounds being potent inhibitors of both phosphodiesterase III and IV, which are useful in the treatment of allergic disorders, atopic diseases and related afflictions. Intermediates in the preparation thereof. Pharmaceutical compositions containing said compounds as an active ingredient. Methods of preparing said compounds and pharmaceutical compositions.

    摘要翻译: PCT No.PCT / EP92 / 02496 Sec。 371日期1994年3月15日 102(e)1994年3月15日PCT提交1992年10月27日PCT公布。 出版物WO93 / 09118 日期:1993年5月13日。新颖的式(I)的1,3-二氢-2H-咪唑并[4,5-b]喹啉-2-酮衍生物其中R是氢,C 1-6烷基,C 3-6环烷基, 任选被1至3个取代基取代的苯基,各自独立地选自卤素,羟基,C 1-6烷氧基,C 5-6环烷氧基,C 1-6烷基或三氟甲基; 吡啶基 任选被卤素或C 1-6烷基取代的噻吩基; C = X =式(C)= O(a),> C = N-O-R1(b)或> C = CH-R2(c)的基团。 其药学上可接受的加成盐和立体化学异构形式,所述化合物是磷酸二酯酶III和IV两者的有效抑制剂,其可用于治疗过敏性疾病,特应性疾病和相关疾病。 中间体在制备中。 含有所述化合物作为活性成分的药物组合物。 制备所述化合物和药物组合物的方法。

    Phenylimidazolidines having antiandrogenic activity
    36.
    发明授权
    Phenylimidazolidines having antiandrogenic activity 失效
    具有抗雄激素活性的苯基咪唑烷

    公开(公告)号:US5411981A

    公开(公告)日:1995-05-02

    申请号:US64257

    申请日:1993-05-18

    摘要: A compound of the formula ##STR1## wherein R.sub.1 is --CN, --NO.sub.2 or halogen, R.sub.2 is --CF.sub.3 or halogen, --A-B-- is of ##STR2## X is --O-- or --S--, R.sub.3 is hydrogen, alkyl, alkenyl or alkynyl of up to 12 carbon atoms, aryl and aralkyl of up to 12 carbon atoms, all optionally substituted by --OH, halogen, --SH, --CN, acyl and acyloxy of up to 7 carbon atoms, --aryl, --O--aryl, --O--aralkyl --S-- aryl of up to 12 carbon atoms the aryl and aralkyl being optionally substituted by halogen, --CF.sub.3, alkyl, alkoxy, alkenyl, alkenyloxy, alkynyl or alkynyloxy with the sulfur being optionally oxidized to sulfone or sulfoxide, free, esterified, amidified or salified carboxy, --NH.sub.2, mono and dialkylamino and heterocyclic of 3 to 6 ring members and containing at least one heteroatom selected from the group consisting of oxygen, sulfur and nitrogen, the alkyl, alkenyl and alkynyl being optionally interrupted by at least one oxygen, nitrogen or sulfur optionally oxidized to sulfoxide or sulfone, trialkylsilyl with the alkyl having 1 to 6 carbon atoms and acyl and acyloxy of an organic carboxylic acid of 1 to 7 carbon atoms and Y is --O--, --S-- or --NH--, except the compounds wherein --A-B-- is ##STR3## X is oxygen, R.sub.3 is hydrogen and Y is oxygen or --NH--, R.sub.2 is --CF.sub.3 or halogen and R.sub.1 is --NO.sub.2 or halogen and their non-toxic, pharmaceutically acceptable acid addition salts.

    摘要翻译: 其中R 1是-CN,-NO 2或卤素,R 2是-CF 3或卤素,-AB-的化合物,其中X是-O-或-S-,R 3是氢,烷基 至多12个碳原子的烯基或炔基,最多12个碳原子的芳基和芳烷基,全部任选被-OH,卤素,-SH,-CN,最多7个碳原子的酰基和酰氧基取代, - 芳基, - 任选被卤素,-CF 3,烷基,烷氧基,烯基,链烯氧基,炔基或炔氧基取代的芳基和芳烷基,其中硫任选被氧化成砜的O-芳基,至多12个碳原子的-O-芳烷基-S-芳基 或亚砜,游离,酯化,酰胺化或盐化的羧基,-NH 2,单和二烷基氨基和3至6个环成员的杂环,并含有至少一个选自氧,硫和氮的杂原子,烷基,烯基和炔基 任选地被至少一个氧,氮或硫任选地中断,所述氧,氮或硫任选地被氧化成亚砜或砜,具有烷基的三烷基甲硅烷基 1至6个碳原子,1至7个碳原子的有机羧酸的酰基和酰氧基,Y为-O - , - S-或-NH-,但其中-AB-为X的化合物为氧, R3是氢,Y是氧或-NH-,R2是-CF3或卤素,R1是-NO2或卤素及其无毒的药学上可接受的酸加成盐。

    Process for absorption of sulfur compounds from fluids
    37.
    发明授权
    Process for absorption of sulfur compounds from fluids 失效
    从流体中吸收硫化合物的工艺

    公开(公告)号:US5342593A

    公开(公告)日:1994-08-30

    申请号:US927584

    申请日:1992-08-10

    摘要: Sulfur dioxide is removed from a fluid containing SO.sub.2 by employing as an absorbent therefor an aqueous solution of compound represented by Formula I: ##STR1## wherein X is --O--, --NR.sup.1 --, or --N.dbd.; each Y is independently --(CR.sup.2.sub.2)--, --(C.dbd.O)--, --O--, --NR.sup.1 --, --N.dbd., or --C(R.sup.2).dbd.; each R.sup.1 or R.sup.2 is independently hydrogen; an alkyl group; a hydroxyalkyl group; an aldehyde group; a carboxylic acid or salt group; or an alkyl group containing an aldehyde group, a carboxylic acid or salt group, ketone, carboxylic ester, ether, or sulfoxide group; and m is an integer preferably of from 2 to about 4. The absorbent solution preferably can be thermally regenerated by heating to remove SO.sub.2.

    摘要翻译: 通过使用式I表示的化合物的水溶液作为吸收剂从含有SO 2的流体中除去二氧化硫:-N =; 每个Y独立地为 - (CR22) - , - (C = O) - , - O - , - NR1 - , - N =或-C(R2) 每个R 1或R 2独立地是氢; 烷基; 羟基烷基; 醛基; 羧酸或盐基; 或含有醛基,羧酸或盐基的烷基,酮,羧酸酯,醚或亚砜基; m优选为2〜4的整数。吸收剂溶液优选通过加热热再生以除去SO 2。