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1. 发明授权

US3928379A N-phenyl amidines 失效
标题翻译： N-苯基脒
公开(公告)号：US3928379A
公开(公告)日：1975-12-23
申请号：US46675374
申请日：1974-05-03
申请人： MEAD JOHNSON & CO
发明人： WU YAO HUA , LOBECK WALTER G
IPC分类号： C07C65/24 , C07D207/08
CPC分类号： C07C65/24 , Y10S514/826
摘要： N-Phenyl amidines which have diuretic, antithrombogenic, smooth muscle relaxant, anti-inflammatory and antiarrhythmic properties have been discovered. They are prepared by reacting a substituted aniline with a carboxamide selected from the group consisting of amides and lactams in the presence of phosphorus oxychloride. Typical examples of substituted N-phenyl amidines thus obtained are 5-methyl-2-(N-phenylbenzylamino)-1-pyrroline, 2-(Nphenylbenzylamino)-1-pyrroline, 3-((N-1-pyrrolin-2-yl-panisidino)methyl)indole and 4,5,6,7,8,9-hexahydro-2-(Nphenylphenethylamino)-3H-azonine. Indole substituted N-phenyl amidines can be rearranged to provide iminopyrrolidinylindoles which are useful as diuretic, antithrombogenic and smooth muscle relaxant agents. In the case of 3-((N-1-pyrrolin-2-yl-panisidino)methyl)indole, the rearranged product is 3-((2-(pmethoxyphenylimino)-1-pyrrolindinyl)methyl)indole.
摘要翻译：已经发现具有利尿，抗血栓形成，平滑肌松弛剂，抗炎和抗心律失常性质的N-苯基脒。它们通过在磷酰氯存在下使取代的苯胺与选自酰胺和内酰胺的羧酰胺反应来制备。由此获得的取代的N-苯基脒的典型实例是5-甲基-2-（N-苯基苄基氨基）-1-吡咯啉，2-（N-苯基苄基氨基）-1-吡咯啉，3 - [（N-1-吡咯啉-2 - 对 - 茴香酰基）甲基]吲哚和4,5,6,7,8,9-六氢-2-（N-苯基苯乙基氨基）-3H-吖嗪。吲哚取代的N-苯基脒可以重排，以提供可用作利尿剂，抗血栓形成剂和平滑肌松弛剂的亚氨基吡咯烷基吲哚。在3 - [（N-1-吡咯啉-2-基 - 对茴香酰基）甲基]吲哚的情况下，重排产物是3 - [[2-（对甲氧基苯基亚氨基）-1-吡咯烷基]甲基]吲哚。

2. 发明授权

US3923886A Sulfamides 失效
标题翻译：磺胺类
公开(公告)号：US3923886A
公开(公告)日：1975-12-02
申请号：US39902473
申请日：1973-09-20
申请人： MEAD JOHNSON & CO
发明人： COMER WILLIAM T , CATT JOHN D
IPC分类号： C07C307/10 , A61K31/18 , A61K31/445 , C07C67/00 , C07C301/00 , C07C303/34 , C07D295/26 , C07C143/76
CPC分类号： C07D295/26 , A61K31/18 , A61K31/445
摘要： Para-Sulfamidophenethanolamines are prepared from parasulfamidophenacyl halides. The phenethanolamines have useful beta-adrenergic blocking action.
摘要翻译：对 - 磺酰胺苯乙酰胺由对 - 磺酰氨基苯甲酰甲酰卤制备。苯乙醇胺具有有用的β-肾上腺素能阻断作用。

3. 发明授权

US3922348A 3{40 ,4{40 -Dihydroxy-2-(isopropylamino)acetophenone intraocular pressure lowering process 失效
标题翻译： 3 {40,4（40-二羟基-2-（异丙基氨基）苯乙酮眼压降低过程
公开(公告)号：US3922348A
公开(公告)日：1975-11-25
申请号：US50663474
申请日：1974-09-16
申请人： MEAD JOHNSON & CO
发明人： SEIDEHAMEL RICHARD J , DUNGAN KENDRICK W
IPC分类号： A61K9/00 , A61K31/135
CPC分类号： A61K31/135 , A61K9/0051
摘要： Topical administration of 3'',4''-dihydroxy-2(isopropylamino)acetophenone to the mammalian eye reduces intraocular pressure without side effects generally associated with adrenergic activation such as tachycardia, mydriasis, hypertension and hypotension.
摘要翻译：向哺乳动物眼睛局部施用3'，4'-二羟基-2-（异丙基氨基）苯乙酮可降低眼内压，而无副作用，通常与肾上腺素能激活相关，如心动过速，散瞳，高血压和低血压。

4. 发明授权

US3919424A Bronchodilator process and composition 失效
标题翻译：支气管扩张剂的过程和组成
公开(公告)号：US3919424A
公开(公告)日：1975-11-11
申请号：US40652473
申请日：1973-10-15
申请人： MEAD JOHNSON & CO
发明人： COMER WILLIAM T , ROTH HERBERT R
IPC分类号： A61K31/18 , A61K31/205 , C07C311/02
CPC分类号： A61K31/18 , A61K31/205 , C07C311/02
摘要： 2''-Hydroxy-5''-(1-hydroxy-2-(2-methyl-1-phenyl-2 -propylamino)ethyl)methanesulfonanilide is a potent anorexigenic agent and orally active bronchodilator.
摘要翻译： 2'-羟基-5' - [1-羟基-2-（2-甲基-1-苯基-2-丙基氨基） - 乙基]甲磺酰苯胺是一种有效的厌食症剂和口服活性支气管扩张剂。

5. 发明授权

US3898342A Phenylimidazolines for producing a neuronal blocking and antihypertensive effect 失效
标题翻译：用于产生神经元阻滞和抗高血压作用的苯基咪唑啉
公开(公告)号：US3898342A
公开(公告)日：1975-08-05
申请号：US47771874
申请日：1974-06-10
申请人： MEAD JOHNSON & CO
发明人： MATIER WILLIAM LESLEY , COMER WILLIAM TIMMEY
IPC分类号： A61K27/00
摘要： The novel compounds of this invention are of the imidazoline class of heterocycles having substituents in the 2 and 4 imidazoline ring positions and optionally in the 3-position. Substituents in the 2-position include amino, hydroxyamino, alkylamino, benzylamino, halobenzylamino, dihalobenzylamino, allylamino, cycloalkylamino, hydrazino, and alkylidenehydrazino. Optional 3-position substituents are alkyl and benzyl. The substituent in the 4-position is comprised of phenyl or R-phenyl in which the R-substituent is selected from halogen, alkyl, benzyloxy, alkoxy, dialkoxy, 3-hydroxy, 3,4-dihydroxy, trifluoromethyl, phenyl, halophenyl, or alkylphenyl. The novel imidazolines have antihypertensive and neuronal blocking properties. They are prepared by cyclization of appropriately substituted 1-phenylethylenediamines with cyanogen bromide or by displacement of a methylmercapto grouping from an appropriately substituted 2-methylthioimidazoline. Representative embodiments of this invention are 2-amino-4-(4-chlorophenyl)-2-imidazoline and 2-amino-4-(3,4-dichlorophenyl)-2-imidazoline.
摘要翻译：本发明的新化合物是在2和4咪唑啉环位置以及任选在3-位具有取代基的咪唑啉类杂环。 2-位的取代基包括氨基，羟基氨基，烷基氨基，苄基氨基，卤代苄基氨基，二卤苄基氨基，烯丙基氨基，环烷基氨基，肼基和亚烷基肼。任选的3-位取代基是烷基和苄基。 4-取代基由苯基或R-苯基组成，其中R取代基选自卤素，烷基，苄氧基，烷氧基，二烷氧基，3-羟基，3,4-二羟基，三氟甲基，苯基，卤代苯基，或烷基苯基。新型咪唑啉具有抗高血压和神经元阻断性能。它们通过用溴化氰环化适当取代的1-苯基乙二胺或通过从适当取代的2-甲硫基咪唑啉置换甲基巯基来制备。本发明的代表性实施方案是2-氨基-4-（4-氯苯基）-2-咪唑啉和2-氨基-4-（3,4-二氯苯基）-2-咪唑啉。

6. 发明授权

US3885047A Ocular hypotensive process employing dextrorotatory phenethanolamines 失效
标题翻译：使用右旋苯乙醇胺的眼压降过程
公开(公告)号：US3885047A
公开(公告)日：1975-05-20
申请号：US42727473
申请日：1973-12-21
申请人： MEAD JOHNSON & CO
发明人： SEIDEHAMEL RICHARD J , DUNGAN KENDRICK W
IPC分类号： A61K9/00 , A61K31/135 , A61K31/18 , A61K27/00
CPC分类号： A61K31/135 , A61K9/0048 , A61K31/18
摘要： Dextrorotatory stereoisomers of beta-adrenergic stimulatory phenethanolamines such as isoproterenol, soterenol, salbutamol, carbuterol, terbutaline, and metaproterenol lower normal or elevated intraocular pressure when topically administered to the eye. Reduction in intraocular pressure is of particular importance in the treatment of glaucoma, a disease marked by ocular hypertension. The dextrorotatory phenethanolamine compounds employed in the process of the present invention are notable for the low order of adrenergic activity in contrast to levorotatory and racemic stereoisomeric forms which are very potent beta-adrenergic stimulatory agents. Consequently, those side effects generally associated with adrenergic activation such as tachycardia, mydriasis, hypertension and hypotension are absent.
摘要翻译：当局部施用于眼睛时，β-肾上腺素能刺激性苯乙醇胺如异丙肾上腺素，异丙肾上腺素，沙丁胺醇，卡特罗特，特布他林和偏多伦他丁的右旋立体异构体降低正常或升高的眼内压。降低眼内压在治疗青光眼中是特别重要的，青光眼是由高眼压症引起的疾病。在本发明方法中使用的右旋苯乙醇胺化合物与非常有效的β-肾上腺素能刺激剂的左旋和外消旋立体异构形式相反，对于肾上腺素能活性的低阶是显着的。因此，通常与肾上腺素能活化相关的副作用如心动过速，散瞳，高血压和低血压都不存在。

7. 发明授权

US3845214A Fertility control process employing ethanolamines 失效
标题翻译：使用乙醇胺的肥料控制过程
公开(公告)号：US3845214A
公开(公告)日：1974-10-29
申请号：US28030372
申请日：1972-08-14
申请人： MEAD JOHNSON & CO
发明人： GALLO D , MAJEWSKI R
IPC分类号： A61K31/13 , A61K31/135 , A61K31/23 , C07C215/08 , C07D295/30 , A01N9/22
CPC分类号： C07D295/30 , C07C243/00 , Y10S514/843
摘要： 1. THE PROCESS FOR REDUCING MAMMALIAN FECUNDITY WHICH COMPRISES ADMINISTERING TO FERTILIZED FEMALE MAMMAL BY THE ORAL OR PARENTERAL ROUTED DURING THE PERIOD FOLLOWING OVULATION AND PRIOR TO THE TIME WHEN IMPLANTATION OCCURS AN EFFECTIVE IMPLANTATION PREVENTING DOSE OF A COMPOUND SELECTED FROM THE GROUP CONSISTING OF A COMPOUND HAVING THE FORMULA

R1-NHCH2CH2-O-R2

WHEREIN R1 IS SELECTED FROM THE GROUP CONSISTING OF LOWER ALKYL HAVING 2 TO 5 CARBON ATOMS INCLUSIVE, LOWER ALKENYL HAVING 3 TO 5 CARBON ATOMS INCLUSIVE, CYCLOALKENYL HAVING 4 TO 5 CARBON ATOMS, CYCLOALKYL HAVING 3 TO 5 CARBON ATOMS INCLUSIVE, DIMETHYLAMINO, PYRROLIDINYL, AND AN ALKYL SUBSTITUTED CYCLOALKYL WHEREIN SAID ALKYL SUBSTITUENT HAS FROM 1 TO 3 CARBON ATOMS INCLUSIVE; AND SAID CYCLOALKYL HAS 3 TO 5 CARBON ATOMS INCLUSIVE; R2 IS SELECTED FROM THE GROUP CONSISTING OF HYDROGEN BENZOYL AND AN ALKANOYL FROM 2 TO 24 CARBON ATOMS INCLUSIVE; OR R1-NH IS PYRROLDDINYL AND A PHARMACEUTICALLY ACCEPTABLE ACID ADDITION SALT OF SAID COMPOUND

8. 发明授权

US3770828A Substituted 3-phenylindan-1-one oximes 失效
标题翻译：取代的3-苯基-1-酮氧化物
公开(公告)号：US3770828A
公开(公告)日：1973-11-06
申请号：US3770828D
申请日：1967-10-20
申请人： MEAD JOHNSON & CO
发明人： BERDAHL J
IPC分类号： A61K31/15 , F16K1/34 , C07C131/00
CPC分类号： A61K31/15
摘要： 3 - (2 - DIMETHYLAMINOETHYL)-3-PHENYLINDAN-I-ONE OXIME PREPARED BY ALKYLATION OF THE DISODIUM SALT OF 3PHENYLINDAN-I-ONE OXIME WITH DIMETHYLAMINOETHYL CHLORIDE IS IDENTICAL WITH THE OXIME PREPARED FROM 3-(2-DIMETHYLAMINO-ETHYL)-3-PHENYLINDAN-1-ONE. THE OXIME HAS STRONG ANTIRESERPINE ACTION.

9. 发明授权

US3723627A Sulfamoyl azide composition and process for lowering blood pressure 失效
标题翻译： SULFAMOYL AZIDE组合物和降低血压的方法
公开(公告)号：US3723627A
公开(公告)日：1973-03-27
申请号：US3723627D
申请日：1970-03-05
申请人： MEAD JOHNSON & CO
发明人： MATIER W , COMER W
IPC分类号： A61K31/18 , C07D295/26 , A61K27/00
CPC分类号： C07D295/26 , A61K31/18
摘要： This invention is concerned with a pharmaceutical process and pharmaceutical compositions for lowering blood pressure in mammals by the administration thereto sulfamoyl azides of the Formula R1R2NSO2N3 and pharmaceutical compositions thereof. R1 is alkyl, cycloalkyl, aryl, aralkyl and so on; R2 is hydrogen, alkyl, cycloalkyl, phenyl, phenylalkyl, and so on; R1 and R2 can be taken together with nitrogen to form a heterocyclic radical.
摘要翻译：本发明涉及通过给予式R 1 R 2 NSO 2 N 3的氨磺酰基叠氮化合物及其药物组合物来降低哺乳动物血压的药物组合物和药物组合物。 R1是烷基，环烷基，芳基，芳烷基等; R2是氢，烷基，环烷基，苯基，苯基烷基等; R1和R2可以与氮一起形成杂环基团。

10. 发明授权

US3651087A Dibenzothiazepine ether intermediates 失效
标题翻译：二苯并噻吩中间体
公开(公告)号：US3651087A
公开(公告)日：1972-03-21
申请号：US1877470
申请日：1970-03-18
申请人： MEAD JOHNSON & CO
发明人： WEBER ABRAHAM , FROSSARD JACQUES JEAN
IPC分类号： C07D281/02 , C07D451/06 , A61K27/00 , C07D93/42
CPC分类号： C07D451/06 , C07D281/02 , Y10S514/869
摘要： NOVEL COMPOUNDS OF FORMULA I HAVING ANTIHISTAMINIC AND OTHER PHARMACOLOGICAL ACTIVITY

11-(Z-O-),5,5-DI(O=),6-R:1,R1,R8,R9-6,11-DIHYDRODIBENZ

(C,F)(1,2)THIAZEPINE

THIS INVENTION IS CONCERNED WITH A NOVEL GROUP OF CHEMICAL SUBSTANCES HAVING ANTIHISTAMINIC AND OTHER PHARMACOLOGIC ACTIVITIES, AND INTERMEDIATES FOR THEIR PREPARATION.

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