Tertiary hydroxyalkylxanthines, medicaments containing them and their use
    1.
    发明授权
    Tertiary hydroxyalkylxanthines, medicaments containing them and their use 失效
    三级羟基烷基黄嘌呤,含有它们的药物及其用途

    公开(公告)号:US4833146A

    公开(公告)日:1989-05-23

    申请号:US32729

    申请日:1987-03-16

    CPC分类号: C07D473/06 C07D473/08

    摘要: Tertiary hydroxyalkylxanthines having the general formula (I), characterized by the fact that at least one of the residues R.sup.1 and R.sup.3 represents a tertiary hydroxyalkyl group of formula (Ia) in which R.sup.4 represents an alkyl group having up to 3 carbon atoms and n a whole number from 2 to 5; the other residue which may remain R.sup.1 or R.sup.3 is a hydrogen atom or an aliphatic hydrocarbon residue R.sup.5 having up to 6 carbon atoms, in which the carbon chain may be separated by a maximum of two oxygen atoms or be substituted by an oxo group or two hydroxy groups at the most, and R.sup.2 represents an alkyl group with 1 to 4 carbon atoms. Also described is a process for manufacturing these compounds, which are suitable for the manufacture of medicines, in particular for use in the prevention and/or treatment of peripheral and/or cerebral irrigation disorders. ##STR1##

    摘要翻译: PCT No.PCT / EP86 / 00401 Sec。 371日期1987年3月16日 102(e)1987年3月16日PCT PCT 1986年7月8日PCT公布。 公开号WO87 / 00523 日本1987年1月29日。具有通式(I)的叔羟基烷基黄嘌呤,其特征在于,残基R 1和R 3中的至少一个表示式(Ia)的叔羟烷基,其中R 4表示具有上述 3个碳原子,na整数2〜5个; 可以保留为R 1或R 3的其它残基是氢原子或具有至多6个碳原子的脂族烃残基R5,其中碳链可以被最多两个氧原子分隔或被氧代基团取代 羟基最多,R 2表示具有1至4个碳原子的烷基。 还描述了一种制备这些化合物的方法,其适用于制备药物,特别是用于预防和/或治疗外周和/或脑灌洗疾病。 (I)(Ia)

    O-Alkylated oximes and pharmaceutical composition thereof
    3.
    发明授权
    O-Alkylated oximes and pharmaceutical composition thereof 失效
    O-烷基化肟及其药物组合物

    公开(公告)号:US4358450A

    公开(公告)日:1982-11-09

    申请号:US63810

    申请日:1979-08-06

    摘要: Compounds of general formula ##STR1## wherein R.sup.1 represents a member selected from the group consisting of (a) an unsubstituted at most binuclear aryl group having from 6 to 10 carbon atoms, such groups substituted by from 1 to 3 equal or different radicals selected from the group consisting of alkyl, halogenoalkyl, alkoxy, dialkylamino each having up to 4 carbon atoms in the alkyl moiety, halogen phenyl, carboxyl, cyano, nitro and hydroxy groups,(b) a 5- to 6-membered heteroaromatic ring wherein the heteroatom is selected from nitrogen, oxygen and sulfur atoms and such rings anellated to a benzene nucleus;R.sup.2 represents a member selected from the group consisting of hydrogen, alkyl having up to 3 carbon atoms, phenyl, cycloalkyl having up to 6 carbon atoms in the ring and cycloalkyl bearing a hydrocarbon bridging radical having up to 2 carbon atoms;R.sup.3 represents hydrogen, hydroxy or acyloxy;R.sup.4 and R.sup.5 are the same or different and each represents a member selected from the group consisting of halogen, alkyl, and halogenoalkyl each having up to 3 carbon atoms, and nitro; andX represents nitrogen or methineand physiologically acceptable acid addition salts thereof and a pharmaceutical composition containing said compounds.

    摘要翻译: 通式(I)的化合物,其中R 1表示选自(a)至少有6至10个碳原子的双核芳基的基团,这些基团被1至3个相等或不同取代的基团 选自烷基部分中具有至多4个碳原子的烷基,卤代烷基,烷氧基,二烷基氨基的基团,卤素苯基,羧基,氰基,硝基和羟基,(b)5-至6-元杂芳环 其中所述杂原子选自氮,氧和硫原子,并且这样的环被安置在苯核上; R2表示选自氢,最多3个碳原子的烷基,苯基,环中具有至多6个碳原子的环烷基和含有至多2个碳原子的烃桥基的环烷基的成员; R3表示氢,羟基或酰氧基; R 4和R 5相同或不同,各自表示选自具有至多3个碳原子的卤素,烷基和卤代烷基的基团,和硝基; X表示氮或次甲基及其生理上可接受的酸加成盐,以及含有所述化合物的药物组合物。

    5-(3-alkyl-5-tert.butyl-4-hydroxyphenyl)-2-amino-6H-1,3,4-thiadiazines
    4.
    发明授权
    5-(3-alkyl-5-tert.butyl-4-hydroxyphenyl)-2-amino-6H-1,3,4-thiadiazines 失效
    5-(3-烷基-5-叔丁基-4-羟基苯基)-2-氨基-6H-1,3,4-噻二嗪

    公开(公告)号:US4940790A

    公开(公告)日:1990-07-10

    申请号:US149601

    申请日:1988-01-28

    CPC分类号: C07D285/16

    摘要: Novel 5-(3-alkyl-5-tert.butyl-4-hydroxyphenyl)-2-amino-6H-1,3,4-thiadiazines of the general formula I ##STR1## in which R.sup.1 =C.sub.1 -C.sub.4 -alkyl,R.sup.2 =H or C.sub.1 -C.sub.3 -alkylR.sup.3 and R.sup.4 =independently of one another, optionally substituted and optionally O- or S-interrupted alkyl, alkenyl or alkynyl groups, it being possible for one of the two radicals to also be H,or R.sup.3 +R.sup.4 together with the nitrogen atom to which they are bound, may denote an optionally substituted 4- to 7-membered ring which optionally contains a further heteroatom (O, S or N),and the physiologically acceptable acid-addition salts thereof. The compounds are primarily suitable for prevention and treatment of inflammatory--in particular inflammatory rheumatic--disorders and/or pain.

    摘要翻译: 通式Ⅰ的新型5-(3-烷基-5-叔丁基-4-羟基苯基)-2-氨基-6H-1,3,4-噻二嗪其中R1 = C1-C4 - 烷基,R 2 = H或C 1 -C 3 - 烷基R 3和R 4彼此独立地是任选取代的,任选地O-或S-间隔的烷基,链烯基或炔基,两个基团之一也可以是 H或R 3 + R 4与它们所连接的氮原子一起可以表示任选取代的4-至7-元环,其任选地含有另外的杂原子(O,S或N)和生理上可接受的酸加成 的盐。 该化合物主要适用于预防和治疗炎症特别是炎性风湿病和/或疼痛。

    Use of xanthine derivatives for the treatment of nerve damage following
an interruption in blood circulation
    5.
    发明授权
    Use of xanthine derivatives for the treatment of nerve damage following an interruption in blood circulation 失效
    黄嘌呤衍生物用于治疗血液循环中断后的神经损伤

    公开(公告)号:US5922868A

    公开(公告)日:1999-07-13

    申请号:US576936

    申请日:1995-12-22

    CPC分类号: C07D473/06

    摘要: Use of xanthine derivatives for the treatment of nerve damage following an interruption in blood circulation.The invention relates to the use of xanthine derivatives of the formula I ##STR1## in which R.sup.2 is a (C.sub.1 -C.sub.4)-alkyl group and at least one of the symbols R.sup.1 and R.sup.3 is a radical of the formula II or III ##STR2## in which A is CHOH, CO or dioxolane, R.sup.4 is a hydrogen atom or a (C.sub.1 -C.sub.4)-alkyl group and n is 0 to 5, and in which R.sup.5 and R.sup.6 are hydrogen atoms or (C.sub.1 -C.sub.4)-alkyl groups or, together with the nitrogen atom to which they are bonded, form a 5- to 7-membered ring, it being possible for one carbon atom to be replaced by an oxygen or nitrogen atom, m is 1 or 2 and the other radical R.sup.1 or R.sup.3, if appropriate, is a hydrogen atom, a (C.sub.1 -C.sub.6)-alkyl group or a (C.sub.3 -C.sub.6)-alkenyl group, for the preparation of medicaments for the prophylaxis and treatment of nerve damage following an interruption in blood circulation, and novel xanthine derivatives, and to processes for their preparation.

    摘要翻译: 黄嘌呤衍生物用于治疗血液循环中断后的神经损伤。 本发明涉及式I的黄嘌呤衍生物,其中R2是(C1-C4) - 烷基,R1和R3中的至少一个是式II或III的基团,其中A是CHOH ,CO或二氧戊环,R4是氢原子或(C1-C4) - 烷基,n是0-5,其中R5和R6是氢原子或(C1-C4) - 烷基,或者与 与它们键合的氮原子形成5-至7-元环,一个碳原子可被氧或氮原子取代,m为1或2,另一个基团R 1或R 3如果合适 是氢原子,(C1-C6) - 烷基或(C3-C6) - 烯基,用于制备用于预防和治疗血液循环中断后的神经损伤的药物,以及新颖的黄嘌呤衍生物 ,以及其准备过程。

    Imidazo- and triazolothiadiazines
    6.
    发明授权
    Imidazo- and triazolothiadiazines 失效
    咪唑并和三唑并噻二嗪

    公开(公告)号:US4891374A

    公开(公告)日:1990-01-02

    申请号:US149546

    申请日:1988-01-28

    摘要: Novel imidazo- and triazolothiadiazines of the general formula I ##STR1## in which R.sup.1 =C.sub.1 -C.sub.4 -alkyl,R.sup.2 =H or C.sub.1 -C.sub.3 -alkyland the structural element --A--B--=--CH.sub.2 --CH.sub.2 --, --CH CH--, --CH.dbd.N--, --CH.sub.2 --CO-- or --CO--CH.sub.2 --,and the physiologically aceptable acid-addition salts thereof, are prepared by reacting 2-halo-1-phenylalkanones of the formula II ##STR2## (meaning of R.sup.1 and R.sup.2 as in formula I, X=halogen) with compounds of the formula III ##STR3## (meaning of --A--B-- as in formula I) and, if appropriate, converting the compounds of the formula I formed into the physiologically acceptable acid-addition salts thereof by means of suitable acids.The compounds of the formula I and the physiologically acceptable acid-addition salts thereof are principally suitable for the prevention and treatment of inflammatory--in particular inflammatory rheumatic--disorders.Some of the intermediates formed during the preparation of the compounds of the formula I are also novel, namely 1-amino-2-mercaptoimidazole ##STR4## and 1-amino-2-thioxo-5-imidazolidinone ##STR5##

    摘要翻译: 其中R 1 = C 1 -C 4 - 烷基,R 2 = H或C 1 -C 3 - 烷基和结构元素-AB - = - CH 2 -CH 2 - , - 的通式I(I)的新型咪唑并 - 和三唑并噻二嗪, CH CH - , - CH = N - , - CH 2 -CO-或-CO-CH 2 - ,及其生理上可接受的酸加成盐,通过使式II的2-卤代-1-苯基烷基酮 (II)(式I中R 1和R 2的含义,X =卤素)与式III化合物(III)(式I中的-AB-的含义)反应,如果合适,将化合物 式I通过合适的酸形成生理上可接受的酸加成盐。 式I化合物及其生理上可接受的酸加成盐主要适用于预防和治疗炎症特别是炎性风湿病。 在制备式I化合物期间形成的一些中间体也是新的,即1-氨基-2-巯基咪唑和1-氨基-2-硫代-5-咪唑啉酮。

    O-[3-(4-Substituted-piperazin-1-yl)-2-hydroxypropyl]-hydroxylamines

    公开(公告)号:US4404384A

    公开(公告)日:1983-09-13

    申请号:US267722

    申请日:1981-05-28

    摘要: A compound of general formula ##STR1## wherein X represents a radical selected from the group consisting of one of the formulae ##STR2## in which R.sup.1 represents a radical selected from the group(a) a hydrogen atom,(b) an amino group, when X represents an --OR.sup.1 moiety,(c) an alkyl group having from 1 to 6 carbon atoms(d) an at most binuclear aryl group being unsubstituted or substituted by at most 3 substituents of the group halogen atoms, alkyl, alkoxy, halogenalkyl groups each having up to 4 carbon atoms, cycloalkyl groups having 3 to 6 carbon atoms, nitro and cyano groups; andR.sup.2 and R.sup.3, which may be the same or different, each represents a radical selected from the group(a) a hydrogen atom,(b) an alkyl group having from 1 to 6 carbon atoms, an unsubstituted cycloalkyl group having from 3 to 7 carbon atoms, such cycloalkyl group substituted by at most 3 substituents of the group hydroxy groups and alkoxycarbonyl groups having 1 to 4 carbon atoms,(c) an aralkyl group, a diaralkyl group each having 1 to 4 carbon atoms in the alkyl moiety and being unsubstituted or substituted in at least one of the radicals in the alkyl moiety by hydroxy groups, and in the aryl moieties by at most 3 substituents selected from the group consisting of alkoxy groups having from 1 to 4 carbon atoms and halogen atoms,(d) an at most binuclear aryl group being unsubstituted or substituted by at most 3 substituents selected from the group consisting of alkyl, alkoxy, halogenoalkyl groups each having up to 4 carbon atoms and halogen atoms,(e) a hydroxy group when the other of R.sup.2 and R.sup.3 is hydrogen,(f) R.sup.2 and R.sup.3, together with the nitrogen atom to which they are attached, represent a 5- to 7-membered ring selected from the group consisting of an unsubstituted ring, a ring being substituted by an alkyl group having from 1 to 4 carbon atoms, and a ring being interrupted by a heteroatom selected from the group consisting of oxygen, sulphur and further nitrogen atom, and(g) R.sup.2 and R.sup.3 together with the nitrogen atom to which they are attached, represent a ring from the group a 5-membered heteroaromatic ring containing up to 4 nitrogen atoms and such a ring being anelled to a benzene- or uracil-ring, and physiologically acceptable acid addition salts thereof, a process for their preparation and a pharmaceutical composition containing them.

    0-(2,3-Epoxypropyl)-hydroximic acid esters
    8.
    发明授权
    0-(2,3-Epoxypropyl)-hydroximic acid esters 失效
    O-(2,3-环氧丙基) - 羟基亚油酸酯

    公开(公告)号:US4150043A

    公开(公告)日:1979-04-17

    申请号:US849935

    申请日:1977-11-09

    IPC分类号: C07D303/12 C07D303/16

    CPC分类号: C07D303/12

    摘要: Compounds of general formula ##STR1## wherein R.sup.1 represents a radical selected from the group consisting of an alkyl group having from 1 to 6 carbon atoms, an unsubstituted aryl group having 6 carbon atoms, an aryl group having 6 carbon atoms being substituted by at least one radical selected from the group consisting of a chlorine atom, alkyl and alkoxy each having up to 2 carbon atoms; and R.sup.2 represents an alkyl group having from 1 to 6 carbon atoms.

    摘要翻译: 通式(I)的化合物,其中R 1表示选自具有1至6个碳原子的烷基,未取代的具有6个碳原子的芳基,具有6个碳原子的芳基被取代的基团 至少一个选自氯原子,烷基和烷氧基中的每一个具有至多2个碳原子的基团; 并且R 2表示具有1至6个碳原子的烷基。

    Imidazolyl-(2)-carbinols having hypolipidemic action and process for
preparing them
    9.
    发明授权
    Imidazolyl-(2)-carbinols having hypolipidemic action and process for preparing them 失效
    具有降血脂作用的咪唑基 - (2) - 甲醇及其制备方法

    公开(公告)号:US4213994A

    公开(公告)日:1980-07-22

    申请号:US6203

    申请日:1979-01-24

    摘要: Pharmaceutical preparations having hypolipidemic activity, which contain in addition to a pharmaceutically acceptable carrier an effective amount of an imidazolyl-(2)-carbinol of the general formula I ##STR1## in which R represents hydrogen, lower alkyl, phenyl or benzyl, R.sub.1 and R.sub.2 each represent hydrogen or together the group --CH.dbd.CH--CH.dbd.CH--, R.sub.3 and R.sub.4 represent hydrogen, lower alkyl, phenyl, lower haloalkyl, lower alkylphenyl, lower alkoxyphenyl, lower haloalkoxyphenyl, mono- or dihalophenyl, imidazolyl or benzylimidazolyl or R.sub.3 and R.sub.4 are together fluoryl of the formula ##STR2## or of a physiologically tolerable acid addition salt thereof, and process for preparing them.

    摘要翻译: 含有降血脂活性的药物制剂,除了药学上可接受的载体之外还含有有效量的通式I(I)的咪唑基 - (2) - 甲醇,其中R表示氢,低级烷基,苯基或苄基 ,R1和R2各自表示氢或基团-CH = CH-CH = CH-,R3和R4表示氢,低级烷基,苯基,低级卤代烷基,低级烷基苯基,低级烷氧基苯基,低级卤代烷氧基苯基,单或二卤代苯基,咪唑基 或苄基咪唑基或R3和R4一起是式“IMAGE”的氟基或其生理上可耐受的酸加成盐,以及其制备方法。

    Novel derivatives of imidazole, and pharmaceutical compositions
containing them
    10.
    发明授权
    Novel derivatives of imidazole, and pharmaceutical compositions containing them 失效
    咪唑的新型衍生物和含有它们的药物组合物

    公开(公告)号:US4152440A

    公开(公告)日:1979-05-01

    申请号:US741418

    申请日:1976-11-12

    摘要: A compound of one of formulae (I) and (II) (of formula sheet) whereinR.sup.1 represents a radical selected from the group consisting of hydrogen alkyl containing up to 6 carbon atoms and being unsubstituted or substituted by at least one of the groups alkoxy and phenylalkoxy containing up to 4 carbon atoms in the alkoxy moiety; aryl or aralkyl each containing from 1 to 4 carbon atoms in the alkyl moiety and being unsubstituted or substituted by at least one substituent selected from the group consisting of alkyl, alkoxy and haloalkyl containing up to 4 carbon atoms, halogen and nitro; a 5- or 6-membered heteroaromatic ring containing up to 2 hetero atoms chosen from O,N and S, at most one of which is different from nitrogen; an alkyl group containing from 1 to 4 carbon atoms substituted by such a heteroaromatic ring;R.sup.2 and R.sup.3, which are the same or different, each represents a hydrogen atom or, alkyl containing up to 4 carbon atoms and being unsubstituted or substituted by at least one substituent selected from the group consisting of alkyl, alkoxy and haloalkyl containing up to 4 carbon atoms, halogen and nitro; taken together R.sup.2 and R.sup.3 alternatively represent a --CH.dbd.CH--CH.dbd.CH-- group which is unsubstituted or substituted by a substituent selected from the group consisting of alkyl, alkoxy and haloalkyl, each containing up to 4 carbon atoms, halogen and nitro;R.sup.4 is selected from the group consisting of hydrogen alkyl, aryl and aralkyl containing up to 4 carbon atoms in each alkyl moiety; andA represents a single bond or alkylene containing from 1 to 6 carbon atoms; with the proviso that R.sup.1 is other than a hydrogen atom or methyl group when A represents a single bond and R.sup.2 and R.sup.3 taken together represent an unsubstituted --CH.dbd.CH--CH.dbd.CH-- group; physiologically acceptable salts thereof, a synthesis therefor and a pharmaceutical composition containing it.

    摘要翻译: 式(I)和(II)之一(式)的化合物,其中R 1表示选自含有至多6个碳原子的烷基的基团,并且是未被取代的或被至少一个烷氧基取代的基团烷氧基 和在烷氧基部分含有至多4个碳原子的苯基烷氧基; 在烷基部分中各自含有1至4个碳原子的芳基或芳烷基,未被取代或被至少一个选自烷基,烷氧基和含有最多4个碳原子的卤代烷基取代的取代基,卤素和硝基; 含有至多2个选自O,N和S的杂原子的5或6元杂芳环,其中最多一个不同于氮; 由这样的杂芳环取代的含有1至4个碳原子的烷基; R 2和R 3相同或不同,各自表示氢原子或含有至多4个碳原子的烷基,未被取代或被至少一个选自烷基,烷氧基和含有至多4个 碳原子,卤素和硝基; 一起取代R2和R3代表-CH = CH-CH = CH-基团,其未被取代或被选自烷基,烷氧基和卤代烷基的取代基取代,每个含有最多4个碳原子的卤素和硝基; R 4选自在每个烷基部分含有至多4个碳原子的烷基,芳基和芳烷基; A表示单键或含有1至6个碳原子的亚烷基; 条件是当A表示单键时,R1不是氢原子或甲基,R2和R3一起代表未取代的-CH = CH-CH = CH-基团; 其生理上可接受的盐,其合成物和含有它的药物组合物。