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51. 发明授权

US3862184A N-substituted-1-(arylsulfinyl and arylsulfonyl)methanesulfonamides 失效
标题翻译： N-取代-1-（芳基磺酰基和芳基磺酰基）甲磺酰胺
公开(公告)号：US3862184A
公开(公告)日：1975-01-21
申请号：US33786673
申请日：1973-03-05
申请人： DOW CHEMICAL CO
发明人： GORALSKI CHRISTIAN T , KLINGLER THOMAS C
IPC分类号： C07D211/96 , C07D295/26 , C07D87/46 , C07C143/78 , C07D29/34
CPC分类号： C07D295/26 , C07D211/96
摘要： IN WHICH R independently is hydrogen (i.e., no substitution on the phenyl ring), lower alkyl, lower alkoxy, halo or trifluoromethyl; x is 1 to 2; n is 1 to 3, and R1 and R2 independently are hydrogen, lower alkyl or phenyl and together with the nitrogen atom form a heterocycle which may contain an oxygen atom as a hetero atom. The compounds are prepared by reacting the corresponding N-substituted-1(arylthio)methanesulfonamide with small, incremental amounts up to substantially equimolar of 30% hydrogen peroxide in glacial acetic acid at 65*-70*C., to obtain the sulfinyl compound, or substantially two equimolar proportions of 30% hydrogen peroxide in glacial acetic acid at reflux temperature to obtain the sulfonyl compound, and recovering the corresponding sulfinyl or sulfonyl product. The compounds are useful as intermediates for making the dihalomethane analogs, the latter being useful as antimicrobials.
The compounds of the formula
摘要翻译：式IV的化合物独立地为氢（即在苯环上不取代），低级烷基，低级烷氧基，卤素或三氟甲基; x为1〜2; n为1〜3，R 1和R 2独立地为氢，低级烷基或苯基，并与氮原子一起形成可含有氧原子作为杂原子的杂环。通过使相应的N-取代-1-（芳硫基）甲磺酰胺与65％-70℃的冰醋酸中的相应的N-取代-1-（芳基硫代）甲磺酰胺与少量的增量量至多等摩尔的30％过氧化氢反应来制备，得到亚磺酰基化合物，或基本上两个等摩尔比例的30％过氧化氢在冰醋酸中的溶液，得到磺酰基化合物，并回收相应的亚磺酰基或磺酰基产物。该化合物可用作制备二卤代甲烷类似物的中间体，后者可用作抗微生物剂。

52. 发明授权

US3853865A N-aminomethyl-2-amino(and 2-amino-methyl)-2-heterocyclic-thioacetamides 失效
标题翻译： N-氨基-2-氨基（和2-氨基甲基）-2-杂环 - 硫代胺
公开(公告)号：US3853865A
公开(公告)日：1974-12-10
申请号：US26602472
申请日：1972-06-26
申请人： SMITHKLINE CORP
发明人： BRENNER L , LOEV B
IPC分类号： A61K31/44 , C07D207/337 , C07D213/59 , C07D215/12 , C07D239/26 , C07D241/12 , C07D277/20 , C07D277/30 , C07D295/12 , C07D413/12 , C07D87/46
CPC分类号： C07D295/12 , A61K31/44 , C07D213/59 , C07D239/26 , C07D241/12 , C07D413/12
摘要： The compounds are N-aminomethyl-2-amino(and 2-aminomethyl)-2heterocyclic-thioacetamides which are inhibitors of gastric acid secretion.
摘要翻译：这些化合物是作为胃酸分泌抑制剂的N-氨基甲基-2-氨基（和2-氨基甲基）-2-杂环 - 硫代乙酰胺。

53. 发明授权

US3852285A Pyrano- and thiopyranoindole derivatives 失效
标题翻译：吡咯烷酮和吡咯烷衍生物
公开(公告)号：US3852285A
公开(公告)日：1974-12-03
申请号：US21762772
申请日：1972-01-13
申请人： AYERST MCKENNA & HARRISON
发明人： DEMERSON C , HUMBER L , DOBSON T , ASSELIN A , JIRKOVSKY I
IPC分类号： C07D209/08 , C07D87/46
CPC分类号： C07D209/08 , Y10S514/925
摘要： Pyranoindole and thiopyranoindole derivatives characterized by having an amino(lower)alkyl radical attached to either or both the 1 and 9 position of a pyrano(3,4-b)indole or thiopyrano(3,4b)indole nucleus are disclosed. The amino portion of the amino(lower)alkyl radical may be further substituted with one or two lower alkyl groups or incorporated into a heterocyclic amine radical. The derivatives having the amino(lower)alkyl radical only at position 1 are further substituted at position 1 and may be optionally substituted at positions 3,4, 5, 6, 7, 8 and 9. The derivatives having the amino(lower)alkyl radical only at position 9 possess two substitutents at position 1 and may be optionally substituted at position 3, 4, 5, 6, 7, and 8. The derivatives having an amino(lower)alkyl radical at both positions 1 and 9 are further substituted at position 1 and may be optionally substituted at positions 3,4,5, 6, 7 and 8. The pyrano- and thiopyranoindole derivatives of this invention are useful antidepressant and antiulcer agents. Methods for the preparation and use of these derivatives are also disclosed.
摘要翻译：公开了以吡喃并吲哚和噻喃并吲哚衍生物为特征的具有连接于吡喃并[3,4-b]吲哚或噻喃并[3,4-b]吲哚核的1位和9位的氨基（低级）烷基。氨基（低级）烷基的氨基部分可进一步被一个或两个低级烷基取代或并入杂环胺基中。仅在位置1具有氨基（低级）烷基的衍生物在1位进一步被取代，并且可以在3,4,5,6,7,8和9位任意被取代。具有氨基（低级）烷基仅在位置9的基团在位置1具有两个取代基，并且可以任选地在3,4,5,6,7和8位被取代。具有位置1和9的氨基（低级）烷基的衍生物被进一步取代在位置1，并且可以任选地在3,4,5,6,7和8位被取代。本发明的吡喃和噻喃并吲哚衍生物是有用的抗抑郁剂和抗溃疡剂。还公开了这些衍生物的制备和使用方法。

54. 发明授权

US3838121A 2-(aminoalkyl-amino)-4-amino thieno(3,2-d)pyrimidines 失效
标题翻译： 2-（氨基甲酰氨基）-4-氨基三苯并（3,2-D）吡啶
公开(公告)号：US3838121A
公开(公告)日：1974-09-24
申请号：US6093370
申请日：1970-08-04
申请人： BOEHRINGER SOHN INGELHEIM
发明人： WOITUN E , NARR B , SCHROTER W
IPC分类号： C07D495/04 , C07D87/46
CPC分类号： C07D495/04 , Y10S514/822
摘要： 2-(AMINOALKYLAMINO)-THIENO(3,2-D)PYRIMIDINES OF THE FORMULA

2-(H2N-A-N(-R2)-),4-(R-N(-R1)-),R3-THIENO(3,2-D)PYRIMIDINE

WHEREIN R AND R1 MAY BE THE SAME OR DIFFERENT AND ARE SELECTED FROM THE GROUP CONSISTING OF HYDROGEN AND STRAIGHT AND BRANCHED ALKYL OF 1 TO 6 CARBON ATOMS AND TAKEN TOGETHER WITH THE NITROGEN ATOM TO WHICH THEY ARE ATTACHED FORM A SATURATED 5 TO 7 MEMBER HETEROCYCLIC RING WHICH CAN OPTIONALLY CONTAIN AN OXYGEN OR NITROGEN HETEROATOM AND MAY BE SUBSTITUTED WITH ALKYL OF 1 TO 6 CARBON ATOMS OR HYDROXYL, R2 IS SELECTED FROM THE GROUP CONSISTING OF HYDROGEN AND STRAIGHT AND BRANCHED ALKYL OF 1 TO 6 CARBON ATOMS, R3 IS SELECTED FROM THE GROUP CONSISTING OF METHYL IN THE 6- OR 7-POSITION AND HYDROGEN AND A IS A STRAIGHT OR BRANCHED ALKYLENE OF 2 TO 10 CARBON ATOMS AND THEIR NON-TOXIC, PHARMACEUTICALLLY ACCEPTABLE ACID ADDITION SALTS WHICH POSSES CARDIOVASCULAR AND SEDATIVE ACTIVITY AND INHIBIT PLATELET AGGREGATION, AND PROCESSES FOR THEIR PREPARATION.

55. 发明授权

US3803143A 6-amino alkylene 6,7-dihydro-5h-dibenzo (b,g),(1,5)thiazocines 失效
标题翻译： 6-氨基亚苄基6,7-二氢-5H-二苯并（B，G），（1,5）噻吩
公开(公告)号：US3803143A
公开(公告)日：1974-04-09
申请号：US6916670
申请日：1970-09-02
申请人： EISAI CO LTD
发明人： TANAKA S , HASHIMOTO K
IPC分类号： C07D267/22 , C07D281/18 , C07D87/46
CPC分类号： C07D281/18 , C07D267/22
摘要： EIGHT-MEMBERED HETEROCYCLIC CMPOUNDS, ESPECIALLY 6SUBSTITUTED 6,7-DIHYDRO-5H-DIBENZO(B,G), (1,5)OXAZOCINE AND CORRESPONDING THIAZOCINE AS WELL AS PHARMACOLOGICALLY ACCEPTABLE SALTS THEREOF HAVING AN OUTSTANDING ANTI-DEPRESSANT ACTIVITY ON THE NERVOUS SYSTEM. THE NEW COMPOUNDS ARE USEFUL FOR THE TREATMENT OF DISEASE SUCH AS DEPRESSIONS, FOR EXAMPLE, DEPRESSIONS CAUSED BY CLIMACTERIC AND MIDDLE-AGED SYNDROMES, ARTERIOSCLEROSIS AND PARKINSON''S DISEASE. THE INVENTION ALSO INVOLVES A PROCESS FOR THE PRODUCTION OF THE COMPOUNDS.

56. 发明授权

US3769283A N-acyl sydnonimine derivatives 失效
标题翻译： N-乙酰基尼龙酮衍生物
公开(公告)号：US3769283A
公开(公告)日：1973-10-30
申请号：US3769283D
申请日：1970-09-14
申请人： TAKEDA CHEMICAL INDUSTRIES LTD
发明人： MASUDA K , IMASHIRO Y
IPC分类号： C07D271/04 , C07D413/12 , C07D87/42 , C07D87/46
CPC分类号： C07D413/12 , C07D271/04 , Y10S514/906 , Y10S514/929
摘要： DERIVATIVES OF THE SYDONIMINES ACCORDING TO U.S. PAT. NO. 3,312,690, WHEREIN THE IMINO GROUP IS REPLACED BY N-FORMYL, N-ACETYL, N-PROPIONYL, N-MONOCHLORO ACETYL, N-DICHLORO ACETYL, N-TRICHLORO ACETYL, N-TRIFLUORO ACETYL, N-PHENOXY ACETYL, N-PHENOXY PROPIONYL, N-PHENYL ACETYL, N-PHENYL PROPIONYL, N-CINNAMOYL, N-BENZOYL, N-ETHOXY CARBONYL, N-BENZYLOXY CARBONYL, N-METHYL, CARBAMOYL, N-ETHYL CARBAMOYL, N-PHENYL CARBAMOYL, N-NICOTINOYL, N-ISONICOTINOYL, N-(N''-CARBOBENZYLOXY ALAYL), NMETHYL SULFONYL, N-PHENYL SULFONYL, N-P-CHLOROPHENYL SULFONYL, N-NITROSO, ETC., AND PHARMACEUTICALLY ACCEPTABLE SALTS THEREOF HAVE SUPERIOR UTILITY AS HYPOTENSIVE DRUGS, CORONARY AND PERIPHERAL VESSEL DILATORS OR MUSCLE RELAXANTS. THE 3-POSITIONED

R1-N(-R2)-GROUP

MAY ALSO BE AN

(ARALKYL)2-N-GROUP

EACH ARALKYL HAVING 7 TO 9 CARBON ATOMS.

57. 发明授权

US3757016A Herbicidal compounds and methods 失效
标题翻译：除草化合物和方法
公开(公告)号：US3757016A
公开(公告)日：1973-09-04
申请号：US3757016D
申请日：1971-07-12
申请人： UNITED STATES BORAX CHEM
发明人： HUNTER D , KITASAKI K , LE FEVRE C
IPC分类号： C07C331/28 , C07D295/18 , C07D295/215 , C07D87/46 , C07D87/42
CPC分类号： C07D295/215 , C07C265/12 , C07C331/28
摘要： A NOVEL CLASS OF COMPOUNDS COMPRISING THE ESTERS OF 2-(W,W-DIETHYLENEIXYURAMIDO) BENZOIC ACID AND THE THIO ANALOGUES THEREOF ARE PROVIDED. THE COMPOUNDS ARE USEFUL AS HERBICIDES AND ARE ESPECIALLY USEFUL FOR CONTROLLING WILD OATS IN THE PRESENCE OF DESIRABLE CROPS.

58. 发明授权

US3755317A Thioamides of 4-substituted syringic acid and their preparation 失效
标题翻译： 4-取代的水杨酸的制备及其制备
公开(公告)号：US3755317A
公开(公告)日：1973-08-28
申请号：US3755317D
申请日：1970-11-27
申请人： ISF SPA
发明人： PIFFERI G
IPC分类号： C07D295/10 , C07D261/02 , C07D263/06 , C07D277/04 , C07D295/18 , C07D295/194 , C07D87/46
CPC分类号： C07D261/02 , C07D277/04 , C07D295/194
摘要： New thioamides of 4-substituted zyringic acid are provided, which are characterized with respect to the corresponding amides in that they have a more prolonged effect. The new thioamides herein provided can be used in therapy showing a prolonged ataraxic or tranquilizing action upon the central nervous system without comprising the reflexes and the motorial coordination; furthermore, they show a very low toxicity, a favourable therapeutic coefficient and the absence of collateral effects on the circle.
摘要翻译：提供了4-取代的丁酸的新的硫代酰胺，其相对于相应的酰胺被表征，因为它们具有更长的效果。本文提供的新型硫代酰胺可用于治疗，显示对中枢神经系统长时间的无痛或镇静作用，不包括反射和运动协调; 此外，它们显示出非常低的毒性，良好的治疗系数和在圆圈上没有附带效应。

59. 发明授权

US3726868A Phenyl and substituted phenylsulfonylallyl amines and substituted amines 失效
标题翻译：苯基和取代的苯基磺酰胺和取代的胺
公开(公告)号：US3726868A
公开(公告)日：1973-04-10
申请号：US3726868D
申请日：1971-09-16
申请人： SANDOZ AG
发明人： MANNING R
IPC分类号： C07D203/08 , C07D295/092 , C07D87/46
CPC分类号： C07D203/08 , C07D295/088
摘要： PHENYL AND SUBSTITUTED PHENYLSULFONYLALLYL AMINES AND SUBSTITUTED AMINES, E.G., 1-(3-PHENYLSULFONYLALLYL$-PYRROLIDINE HYDROCHLORIDE, ARE PREPARED BY TREATING A PHENYL OR SUBSTITUTED PHENYLSULFONYL-2-PROPEN-1-OL WITH AN AMINE OR SUBSTITUTED AMINE, TREATING THE RESULTING INTERMEDIATE WITH SOCL2 AND THEN WITH SODIUM CARBONATE AND ALLOWING THE RESULTING INTERMEDIATE TO REARRANGE TO THE FINAL PRODUCT. THE COMPOUNDS ARE USEFUL AS ANTI-INFLAMMATORY AGENTS.

60. 发明授权

US3726866A 2-benzimidazalyldithio carbamates 失效
标题翻译： 2-BENZIMIDAZALYLDITHIO CARBAMATES
公开(公告)号：US3726866A
公开(公告)日：1973-04-10
申请号：US3726866D
申请日：1970-11-02
申请人： MONSANTO CO
发明人： D AMICO J
IPC分类号： C07D233/42 , C07D233/84 , C07D235/28 , C07D239/38 , C08K5/39 , C07D87/46
CPC分类号： C07D239/38 , C07D233/42 , C07D233/84 , C07D235/28 , C08K5/39 , C08L21/00
摘要： Heterocyclic esters of dithiocarbamic acid wherein the heterocycle is 2-imidazolyl, 2-imidazolinyl, 2-benzimidazolyl, or substituted derivatives thereof which esters are useful for accelerating the vulcanization of rubber.

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