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    Treatment of psychic disorders and inflammation with fused isoquinolines
    1.
    发明授权
    Treatment of psychic disorders and inflammation with fused isoquinolines 失效
    治疗心理障碍和炎症与融合异喹啉

    公开(公告)号：US4232017A

    公开(公告)日：1980-11-04

    申请号：US41356

    申请日：1979-05-22

    申请人： Giorgio Winters ,  Nunzio Di Mola

    发明人： Giorgio Winters ,  Nunzio Di Mola

    IPC分类号： A61K31/47 ,  A61P25/20 ,  A61P29/00 ,  C07D231/38 ,  C07D471/04 ,  C07D513/04 ,  A61K31/54

    CPC分类号： C07D231/38 ,  C07D471/04 ,  C07D513/04

    摘要： New tricyclic ortho-fused heterocyclic compounds of formula ##STR1## wherein A is the group ##STR2## or the group ##STR3## in which R represents hydrogen, (C.sub.1-4)alkyl, phenyl or tolyl and R.sub.1 and may be (C.sub.1-4)alkyl, phenyl or tolyl, R.sub.2 is selected from (C.sub.1-4)alkyl, (C.sub.2-4)alkanoylmethyl, carbo(C.sub.1-3)alkoxymethyl, hydroxy(C.sub.2-4)alkyl, halo(C.sub.2-4)alkyl and a group ##STR4## wherein R.sub.3 is an alkylene group from 2 to 4 carbon atoms and R.sub.4 and R.sub.5 independently represent hydrogen or (C.sub.1-4)alkyl or, taken together with the nitrogen atom, a fully hydrogenated 5 or 6 membered heterocyclic radical which may contain a further heteroatom selected from O, N and S and be optionally substituted by a (C.sub.1-4)alkyl or phenyl group, or R.sub.2 may represent, nil the dotted lines x and y may represent nil or additional bonds; with the proviso that, when the symbol R.sub.2 linked to the oxygen atom is different from nil, x is an additional bond and y and the other symbol R.sub.2 represent nil; with the further proviso that, when the symbol R.sub.2 linked to the nitrogen atom is different from nil, y is an additional bond and x and the other symbol R.sub.2 represent nil; and salts therewith of pharmaceutically acceptable acids. The compounds possess antiinflammatory, CNS-depressent and anti-anxiety utility.

    摘要翻译： 新的式（I）所示的三环邻 - 稠合杂环化合物，其中A为基团（a）或基团（b），其中R表示氢，（C 1-4）烷基，苯基或甲苯基， R1可以是（C1-4）烷基，苯基或甲苯基，R2选自（C1-4）烷基，（C2-4）烷酰基甲基，碳（C1-3）烷氧基甲基，羟基（C2-4） （C 2-4）烷基和基团，其中R 3是2至4个碳原子的亚烷基，且R 4和R 5独立地表示氢或（C 1-4）烷基，或者与氮原子一起完全氢化 5或6元杂环基，其可以含有选自O，N和S的另外的杂原子，并且任选地被（C 1-4）烷基或苯基取代，或者R 2可以表示，虚线x和y可以表示nil 或附加债券; 条件是当连接到氧原子的符号R2不同于nil时，x是附加键，y和其它符号R2表示nil; 进一步的条件是当连接到氮原子的符号R2不同于nil时，y是附加键，x和其它符号R2表示nil; 以及其与药学上可接受的酸的盐。 该化合物具有抗炎，CNS抑制和抗焦虑效用。

    Antiinflammatory 2-imino-indolines and their pharmaceutical compositions
    2.
    发明授权
    Antiinflammatory 2-imino-indolines and their pharmaceutical compositions 失效
    抗炎2-亚氨基 - 吲哚啉及其药物组合物

    公开(公告)号：US3984563A

    公开(公告)日：1976-10-05

    申请号：US504205

    申请日：1974-09-09

    申请人： Giorgio Winters ,  Nunzio Di Mola

    发明人： Giorgio Winters ,  Nunzio Di Mola

    IPC分类号： B01J27/00 ,  C07B61/00 ,  C07C243/36 ,  C07D209/40 ,  C07D209/96 ,  C07D209/14 ,  A61K31/40

    CPC分类号： C07C243/00 ,  C07C243/36 ,  C07D209/40 ,  C07D209/96

    摘要： Compounds with antiinflammatory, analgesic and CNS depressant activity having the following general formula ##SPC1##WhereinR represents hydrogen or methoxy;R.sub.1 represents hydrogen; lower alkyl; lower alkyl substituted with a group carboxy, carbo(lower alkoxy) or carbamyl; phenyl; benzyl, lower aliphatic acyl; benzoyl; benzoyl substituted with a halo group;R.sub.2 represents hydrogen; lower alkyl; carbo(lower alkoxy); carbamyl; phenylcarbamyl; lower aliphatic acyl; benzoyl; benzoyl substituted with a halo group,R.sub.3 represents halo; lower alkyl; lower alkyl substituted with a group selected from carboxy, carbo(lower alkoxy), carbamyl, halo, amino, mono and di-lower alkylamino, phthalimido and morpholino; phenyl; phenyl substituted with a group selected from lower alkoxy, halo, nitro, amino and acetamido;R.sub.4 represents hydrogen or lower alkyl; with the proviso that when simultaneously R.sub.1 represents hydrogen, methyl, phenyl, benzyl, acetyl or benzoyl, R.sub.2 represents hydrogen, lower alkyl or acetyl,R.sub.3 represents lower alkyl or phenyl, R.sub.4 must be different from hydrogen and methyl;Or R.sub.3 and R.sub.4 taken together with the adjacent carbon atom may represent a 5-6 membered alicyclic ring.

    摘要翻译： 具有抗炎，镇痛和CNS抑制活性的化合物具有以下通式，其中R表示氢或甲氧基; R1表示氢; 低级烷基 被羧基取代的低级烷基，碳（低级烷氧基）或氨基甲酰基; 苯基; 苄基，低级脂族酰基; 苯甲酰 用卤代基取代的苯甲酰基; R2表示氢; 低级烷基 碳（低级烷氧基）; 氨基甲酰 苯基氨基甲酰基; 低级脂肪族酰基; 苯甲酰 被卤素取代的苯甲酰基，R3代表卤素; 低级烷基 被选自羧基，碳（低级烷氧基），氨基甲酰基，卤素，氨基，单和二低级烷基氨基，苯二甲酰亚氨基和吗啉代的基团取代的低级烷基; 苯基; 被选自低级烷氧基，卤素，硝基，氨基和乙酰氨基的基团取代的苯基; R4代表氢或低级烷基; 条件是当R 1代表氢，甲基，苯基，苄基，乙酰基或苯甲酰基时，R 2表示氢，低级烷基或乙酰基，R 3表示低级烷基或苯基，R 4必须不同于氢和甲基; OR 3和R 4与相邻碳原子一起可以表示5-6元脂环。

    Pharmacologically active pyrazolopyridines
    3.
    发明授权
    Pharmacologically active pyrazolopyridines 失效
    药理活性吡唑并吡啶

    公开(公告)号：US4954508A

    公开(公告)日：1990-09-04

    申请号：US286917

    申请日：1988-12-20

    申请人： Giorgio Winters

    发明人： Giorgio Winters

    IPC分类号： A61K31/435 ,  A61P3/00 ,  A61P3/14 ,  A61P9/08 ,  A61P9/12 ,  A61P43/00 ,  C07D471/04

    CPC分类号： C07D471/04

    摘要： The present invention is directed to new 4,7-dihydro-pyrazolo[3,4-b]pyridines. The compounds possess Ca.sup.2+ -antagonist, antihypertensive, vasodilating and antiangina activity. A process for producing them as well as pharmaceutical compositions containing them are also described.

    摘要翻译： 本发明涉及新的4,7-二氢 - 吡唑并[3,4-b]吡啶。 该化合物具有Ca2 + - 拮抗剂，抗高血压，血管舒张和抗血管活性。 还描述了制备它们的方法以及含有它们的药物组合物。

    Fused isoquinoline derivatives
    6.
    发明授权
    Fused isoquinoline derivatives 失效
    稠油异喹啉衍生物

    公开(公告)号：US4113731A

    公开(公告)日：1978-09-12

    申请号：US713011

    申请日：1976-08-09

    申请人： Giorgio Winters ,  Nunzio DiMola

    发明人： Giorgio Winters ,  Nunzio DiMola

    IPC分类号： C07D209/40 ,  C07D231/38 ,  C07D277/48 ,  C07D471/04 ,  C07D491/048 ,  C07D513/04 ,  C07D471/14 ,  C07D495/14 ,  C07D513/14

    CPC分类号： C07D231/38 ,  C07D209/40 ,  C07D277/48 ,  C07D471/04 ,  C07D513/04

    摘要： Fused isoquinoline derivatives of the general formula ##STR1## wherein: A is a divalent radical selected from the groups ##STR2## wherein R.sub.3 and R.sub.4 each independently represents hydrogen, alkyl,, alkenyl, cycloalkyl, aryl, aralkyl, aralkenyl, cycloalkyl-alkyl or, taken together with the adjacent double bond, represent a cycloalkene containing from 5 to 8 carbon atoms or an aromatic nucleus;R.sub.5 represents hydrogen, hydroxyl, alkyl, alkenyl, cycloalkyl, aryl, aralkyl, aralkenyl or cycloalkyl-alkyl;Y is .dbd.O, .dbd.S or .dbd.NH;X is --O--, --S-- or --NR.sub.6 -- wherein R.sub.6 represents hydrogen, alkyl, cycloalkyl, aryl, aralkyl or cycloalkyl-alkyl;R.sub.1 and R.sub.2 each independently represents hydrogen, alkyl, phenyl, cycloalkyl, alkoxy, alkenyloxy, methylenedioxy, cycloalkoxy, halo or di-alkylamino or, taken together with the adjacent carbon atoms of the benzene ring, form a cycloalkenyl group containing 5 or 6 carbon atoms or an aromatic nucleus fused on the benzene ring. The compounds are essentially prepared through thermal cyclization of a compound of the formula ##STR3## wherein A, X, Y, R.sub.1 and R.sub.2 have the same meanings given before, with the proviso that R.sub.1 and R.sub.2 cannot simultaneously occupy both the ortho positions, B represents hydrogen, R represents an --OR.sub.7 or --NR.sub.8 R.sub.9 radical wherein R.sub.7 is alkyl, aryl or aralkyl and R.sub.8 and R.sub.9 each independently represents hydrogen, alkyl, aryl, aralkyl, or taken together with the adjacent nitrogen atom represent a heterocyclic saturated radical of 5 or 6 atoms which may contain a further hetero-atom selected from oxygen and nitrogen, or the symbols B and R taken together represent a further bond between the adjacent carbon and nitrogen atoms.

    摘要翻译： 通式（I）的稠合异喹啉衍生物其中：A是选自下组的二价基团，其中R 3和R 4各自独立地表示氢，烷基，烯基，环烷基，芳基，芳烷基，芳烯基，环烷基 或与相邻双键一起代表含有5-8个碳原子的环烯烃或芳族核; R5表示氢，羟基，烷基，烯基，环烷基，芳基，芳烷基，芳烯基或环烷基 - 烷基; Y = O，= S或= NH; X是-O - ， - S-或-NR 6 - ，其中R 6表示氢，烷基，环烷基，芳基，芳烷基或环烷基 - 烷基; R 1和R 2各自独立地表示氢，烷基，苯基，环烷基，烷氧基，烯氧基，亚甲二氧基，环烷氧基，卤代或二烷基氨基，或与苯环的相邻碳原子一起形成含有5或6个碳的环烯基 原子或稠合在苯环上的芳香核。 这些化合物基本上通过式（VI）化合物的热环化制备，其中A，X，Y，R 1和R 2具有以下相同的含义，条件是R 1和R 2不能同时占据邻位 位置，B表示氢，R表示-OR7或-NR8R9基，其中R7为烷基，芳基或芳烷基，R8和R9各自独立地表示氢，烷基，芳基，芳烷基或与相邻氮原子一起表示杂环饱和 可以含有另一个选自氧和氮的杂原子的5或6个原子的基团，或符号B和R一起代表相邻的碳原子和氮原子之间的另外的键。

    2-Phenyl-pyrazolo-[1,5-a]quinoline compounds
    7.
    发明授权
    2-Phenyl-pyrazolo-[1,5-a]quinoline compounds 失效
    2-苯基 - 吡唑并 - {8,1-a {9喹啉化合物

    公开(公告)号：US4024149A

    公开(公告)日：1977-05-17

    申请号：US624614

    申请日：1975-10-22

    申请人： Giorgio Winters ,  Gianfranco Odasso ,  Giulio Galliani ,  Leonard J. Lerner

    发明人： Giorgio Winters ,  Gianfranco Odasso ,  Giulio Galliani ,  Leonard J. Lerner

    IPC分类号： C07D249/08 ,  C07D471/04 ,  C07D487/04

    CPC分类号： C07D249/08 ,  C07D471/04

    摘要： New heterocyclic compounds represented by the following formula: ##STR1## wherein: R and R.sub.1 are independently selected from hydrogen, hydroxy, (C.sub.1-4)alkyl, (C.sub.1-4)alkoxy, (C.sub.3-5)alkenyloxy, (C.sub.3-5)alkynyloxy, (C.sub.3-6)cycloalkyloxy, or halo or taken together represent a methylenedioxy group; the symbols W and A are defined as follows:1. W is the nitrogen atom and A is the group ##STR2## in which the carbon atom bearing the radical R.sub.2 is linked to the benzene ring and R.sub.2 is hydrogen, hydroxy, (C.sub.1-4)alkoxy or (C.sub.2-4)aliphatic acyloxy;2. W is the group =CH-- and A is --CH.sub.2 --, --CH.sub.2 --CH.sub.2 -- or --CH=CH--.The compounds have antireproductive utility.

    摘要翻译： 由下式表示的新的杂环化合物：其中：

    Water soluble esters of steroid-oxazole and pharmaceutical compositions containing them
    9.
    发明授权
    Water soluble esters of steroid-oxazole and pharmaceutical compositions containing them 失效
    类固醇恶唑的水溶性酯和含有它们的药物组合物

    公开(公告)号：US4440764A

    公开(公告)日：1984-04-03

    申请号：US258098

    申请日：1981-04-27

    申请人： Giangiacomo Nathansohn ,  Giorgio Winters

    发明人： Giangiacomo Nathansohn ,  Giorgio Winters

    IPC分类号： A61K31/58 ,  A61P5/38 ,  C07J71/00

    CPC分类号： C07J71/0068 ,  Y10S514/885 ,  Y10S514/921

    摘要： Water-soluble esters of steroid-oxazole derivatives of formula I ##STR1## wherein R is O or a H, (.beta.-OH) group, R.sub.1 is hydrogen, lower alkyl or phenyl, X is hydrogen, fluorine or chlorine, A stands for a direct carbon-carbon bond or a hydrocarbon chain containing from 1 to 4 carbon atoms, and M is hydrogen or a pharmaceutically acceptable cation are described as well as pharmaceutical compositions containing them particularly suitable for parenteral administration.

    摘要翻译： 式I的类固醇 - 恶唑衍生物的水溶性酯其中R为O或H，（β-OH）基团，R 1为氢，低级烷基或苯基，X为氢，氟或氯，A为 对于直接碳 - 碳键或含有1至4个碳原子的烃链，并且M是氢或药学上可接受的阳离子以及含有它们的药物组合物，特别适合于肠胃外给药。