2'-(Orthochlorobenzoyl)-4'-chloroglycylanilides, compositions thereof,
and use as medicaments
    2.
    发明授权
    2'-(Orthochlorobenzoyl)-4'-chloroglycylanilides, compositions thereof, and use as medicaments 失效
    2' - (邻氯苯甲酰基)-4'-氯草酰酰苯胺及其组合物,并用作药物

    公开(公告)号:US4382930A

    公开(公告)日:1983-05-10

    申请号:US220514

    申请日:1980-12-29

    摘要: The present invention relates to 2'-(ortho-chlorobenzoyl)-4'-chloroglycylanilides, compositions thereof, and their use as medicaments, e.g., as anxiolytic agents.The compounds of the invention have the general formula I ##STR1## in which R represents hydrogen or alkyl,R.sub.1 and R.sub.2 may be identical or different and are selected from hydrogen, alkyl, hydroxyalkyl, alkenyl, and alkynyl, possibly substituted by alkyl, and cycloalkyl having three to six members, possibly substituted by alkyl, with the proviso that, when one of R.sub.1 and R.sub.2 represents hydrogen, the other is not lower alkyl or hydroxyalkyl; and with the further proviso that R.sub.1 and R.sub.2 may not simultaneously represent either hydrogen or lower-alkyl. R.sub.1 and R.sub.2 may furthermore form, with the nitrogen atom to which they are connected, a nitrogen heterocycle possibly containing a second heteroatom selected from oxygen and nitrogen.

    摘要翻译: 本发明涉及2' - (邻氯苯甲酰基)-4'-氯草酰苯胺,其组合物及其作为药物的用途,例如作为抗焦虑剂。 本发明的化合物具有通式I(I)其中R表示氢或烷基,R 1和R 2可以相同或不同,并且选自氢,烷基,羟基烷基,烯基和炔基,可能被 烷基和具有3至6个成员的环烷基,可能被烷基取代,条件是当R 1和R 2之一表示氢时,另一个不是低级烷基或羟烷基; 并且进一步的条件是R 1和R 2可以不同时表示氢或低级烷基。 R1和R2可以与它们所连接的氮原子形成可能含有选自氧和氮的第二杂原子的氮杂环。

    Method of treating hyperuricemia and gout
    3.
    发明授权
    Method of treating hyperuricemia and gout 失效
    治疗高尿酸血症和痛风的方法

    公开(公告)号:US4271191A

    公开(公告)日:1981-06-02

    申请号:US105420

    申请日:1979-12-19

    申请人: France Mazoyer

    发明人: France Mazoyer

    摘要: The present application relates to the treatment of hyperuricemias, including the prevention and treatment of gout, using the compound Itanoxone or a pharmaceutically-acceptable salt thereof. The compound Itanoxone has the chemical name 2'-chloro-4,4-biphenyl-4-oxo-2-methylene-butyric acid, and may alternatively be named 2-methylene 4-oxo 4-(4'-ortho-chlorophenylphenyl)-butyric acid. The formula for the compound is as follows: ##STR1##The international common name of this compound is "Itanoxone". Pharmaceutical compositions of the active ingredient, suitable for carrying out the method of the invention, and combinations thereof with other active ingredients, particularly colchicine and allopurinal, are also disclosed.

    摘要翻译: 本申请涉及使用化合物伊立诺酮或其药学上可接受的盐治疗高尿酸血症,包括预防和治疗痛风。 化合物伊立诺酮具有化学名称2'-氯-4,4-联苯-4-氧代-2-亚甲基丁酸,或者可以将其称为2-亚甲基-4-氧代-4-(4'-邻氯苯基苯基) - 丁酸。 该化合物的配方如下:

    .beta.-Nicotinamido-ethyl anthranilate
    4.
    发明授权
    .beta.-Nicotinamido-ethyl anthranilate 失效
    乙酰氨基苯甲酸乙酯

    公开(公告)号:US4152521A

    公开(公告)日:1979-05-01

    申请号:US931488

    申请日:1978-08-07

    IPC分类号: C07D213/82 C07D213/56

    CPC分类号: C07D213/82

    摘要: The invention concerns new chemical compounds which can be used as medicaments, their preparation, and pharmaceutical compositions, and method of treating therewith.The new chemical compounds have the general formula ##STR1## in which X, which is in 7 position, represents a halogen atom or a trifluoromethyl group.The medicaments containing these active principles may be used in the treatment of various pains, i.e., as analgesics.

    摘要翻译: 本发明涉及可用作药物的新化合物,其制备方法和药物组合物及其处理方法。

    Process for obtaining a plasminogen activator
    5.
    发明授权
    Process for obtaining a plasminogen activator 失效
    获得纤溶酶原激活物的方法

    公开(公告)号:US3998947A

    公开(公告)日:1976-12-21

    申请号:US529147

    申请日:1974-12-03

    摘要: A process for obtaining a plasminogen activator involves treating an acetone extract powder of organs of animals, such as the lungs and kidneys of pigs, calves, bullocks, horses, lambs or sheep or the ovaries of porcine, bovine or ovine animals, by suspension in an aqueous saline solution, taking up the precipitate obtained in an aqueous saline solution of greater ionic strength and lower pH-value, decanting the solution and precipitating therefrom at acidic pH by adding a salt or an organic solvent, further taking up the precipitate obtained in water or a saline solution, followed by repeated precipitation by adding a salt at a somewhat higher pH-value, finally taking up the precipitate obtained in water and dialyzing the solution, and optionally purifying the solution obtained.The activator obtained may be used as a medicament.

    摘要翻译: 用于获得纤溶酶原激活剂的方法包括通过将悬浮于牛血清中的动物的器官例如猪,小牛,牛,马,羔羊或绵羊或猪,牛或绵羊动物的卵巢的肺和肾脏的丙酮提取物粉末 吸收在离子强度较高和pH值较低的盐水溶液中获得的沉淀物,倾倒溶液,并通过加入盐或有机溶剂,在酸性pH下从其中沉淀出来,进一步吸收在 水或盐水溶液,然后通过在稍高的pH值下加入盐重复沉淀,最后吸收在水中得到的沉淀物并透析溶液,并任选地纯化所得溶液。

    Derivatives of phenoxy isobutyric acid having hypolipemizing and
hypocholesterolemizing action
    6.
    发明授权
    Derivatives of phenoxy isobutyric acid having hypolipemizing and hypocholesterolemizing action 失效
    具有高效和高脂肪氧化活性的苯氧基异丁酸的衍生物

    公开(公告)号:US3987175A

    公开(公告)日:1976-10-19

    申请号:US577402

    申请日:1975-05-14

    申请人: Henri Cousse

    发明人: Henri Cousse

    CPC分类号: C07D213/82 C07D213/89

    摘要: The present invention relates to new chemical products which are useful as hypolipemizing and hypocholesterolemizing agents.The new compounds are derivatives of phenoxy isobutyric acid of the general formula ##EQU1## wherein: A is a lower-alkylene bridge of 2 to 6 carbon atoms, either linear or branched,X is a halogen atom,R = h or lower-alkyl,The N of the pyridyl ring can be replaced by an N-oxide, or the compounds can be in the form of their pharmaceutically-acceptable acid addition salts.Pharmaceutical compositions containing these active principles are useful for hypolipemizing and hypocholesterolemizing purposes, e.g., in the prevention and treatment of atherosclerosis and its consequences.

    1-Aryl 2-aminomethyl cyclopropane carboxylates (Z)
    8.
    发明授权
    1-Aryl 2-aminomethyl cyclopropane carboxylates (Z) 失效
    2-芳基2-氨基甲基环丙烷羧酸酯(Z)

    公开(公告)号:US4567288A

    公开(公告)日:1986-01-28

    申请号:US656443

    申请日:1984-10-01

    摘要: The present invention concerns new derivatives of 1-aryl 2-aminomethyl cyclopropane carboxylates (Z), their preparation and their use as useful drugs for the treatment of various pains.The new derivatives of the present invention have the general formula I ##STR1## in which: R represents a hydrogen or halogen atom, a C.sub.1 to C.sub.4 lower alkyl group, a C.sub.1 to C.sub.4 lower alkoxy group, or a nitro, amino, sulfamoyl or hydroxy group;n represents the values 1, 2 or 3;(R).sub.n may together with the benzene ring also form the naphthyl group;R.sub.1 represents a linear or branched C.sub.1 to C.sub.5 alkyl or alkenyl group or an aryl or benzyl group;R.sub.2 and R.sub.3 represent a hydrogen atom, a linear or branched C.sub.1 to C.sub.5 alkyl, alkenyl, alkynyl, hydroxyalkyl, alkoxyalkyl, carboxyalkyl or dialkylaminoalkyl group or an aryl, arylalkyl or cycloalkyl group;R.sub.2 and R.sub.3 possibly also forming a heterocycle of 5 or 6 members with the adjacent nitrogen atom,provided however that when R.sub.1 represents the ethyl radical and R represents a hydrogen atom, R.sub.2 and R.sub.3 cannot simultaneously represent a methyl radical.

    摘要翻译: 本发明涉及1-芳基2-氨基甲基环丙烷羧酸酯(Z)的新衍生物,其制备及其作为治疗各种疼痛的有用药物的用途。 本发明的新衍生物具有通式I(I),其中:R表示氢或卤素原子,C1至C4低级烷基,C1至C4低级烷氧基或硝基,氨基 ,氨磺酰基或羟基; n表示值1,2或3; (R)n可以与苯环一起形成萘基; R1表示直链或支链C1至C5烷基或烯基或芳基或苄基; R2和R3表示氢原子,直链或支链C1至C5烷基,烯基,炔基,羟基烷基,烷氧基烷基,羧基烷基或二烷基氨基烷基或芳基,芳烷基或环烷基; R2和R3也可能与相邻的氮原子形成5或6个成员的杂环,但是当R1表示乙基且R表示氢原子时,R2和R3不能同时代表甲基。

    Preparation of 3-amino-1-[(1,4-benzodioxan)-2-yl-methoxy]-2-propanols
    9.
    发明授权
    Preparation of 3-amino-1-[(1,4-benzodioxan)-2-yl-methoxy]-2-propanols 失效
    制备3-氨基-1 - [(1,4-苯并二恶烷)-2-基 - 甲氧基] -2-丙醇

    公开(公告)号:US4539413A

    公开(公告)日:1985-09-03

    申请号:US455125

    申请日:1983-01-03

    CPC分类号: C07D319/20 Y10S514/821

    摘要: The present invention concerns a novel process for the production of new chemical compounds of the general formula: ##STR1## in which: R.sub.1 and R.sub.2 may be identical or different and represent a hydrogen or halogen atom or else a lower alkyl, lower alkoxy, nitro or acetyl group andR represents a lower alkyl or lower aralkyl group, such as benzyl.These compounds are useful in therapy for the treatment of hypertension and cardiac arrhythmia.The novel process involves reaction of a 2-hydroxymethyl-1,4-benzodioxan with epichlorohydrin to produce an intermediate glycidyl ether, which is then reacted with a primary amine to produce the final 3-amino-1-[(1,4-benzodioxan)-2-yl-methoxy]-2-propanol or an acid addition salt thereof.

    摘要翻译: 本发明涉及一种制备通式如下的新化合物的新方法:其中:R 1和R 2可以相同或不同,表示氢或卤素原子,或低级烷基,低级 烷氧基,硝基或乙酰基,R表示低级烷基或低级芳烷基,例如苄基。 这些化合物可用于治疗高血压和心律失常的治疗。 该新方法涉及2-羟甲基-1,4-苯并二恶烷与表氯醇的反应以产生中间体缩水甘油醚,然后将其与伯胺反应以产生最终的3-氨基-1 - [(1,4-苯并二恶烷) )-2-基 - 甲氧基] -2-丙醇或其酸加成盐。

    2-N-Cycloalkylmethyl 3-oxo 5,6-diaryl-as-triazines
    10.
    发明授权
    2-N-Cycloalkylmethyl 3-oxo 5,6-diaryl-as-triazines 失效
    2-N-环烷基甲基3-氧代5,6-二芳基 - 三嗪

    公开(公告)号:US4511566A

    公开(公告)日:1985-04-16

    申请号:US600473

    申请日:1984-04-16

    摘要: The present invention concerns new 2-N-cycloalkylmethyl 3-oxo 5,6-diaryl as-triazines, their method of production, pharmaceutical compositions thereof, and their use as medicaments, for treating pain.The derivatives of 2-N-cycloalkylmethyl 3-oxo 5,6-diaryl as-triazine according to the invention have the general formula I ##STR1## in which Ar represents a phenyl, furyl, thienyl, or pyridyl group, which group may possibly be substituted by a lower C.sub.1 to C.sub.4 alkoxy radical, in particular by the methoxy radical, andn is a whole number having a value of 1 to 4.

    摘要翻译: 本发明涉及新的2-N-环烷基甲基3-氧代5,6-二芳基三嗪,它们的制备方法,其药物组合物及其作为药物的用途,用于治疗疼痛。 根据本发明的2-N-环烷基甲基3-氧代5,6-二芳基 - 三嗪的衍生物具有通式I(I),其中Ar表示苯基,呋喃基,噻吩基或吡啶基,其中 基团可能被低级C1至C4烷氧基取代,特别是被甲氧基取代,n为整数,其值为1至4。