公开(公告)号：US3914249A

公开(公告)日：1975-10-21

申请号：US41110473

申请日：1973-10-30

申请人： MEAD JOHNSON & CO

发明人： MATIER WILLIAM L ,  COMER WILLIAM T

IPC分类号： C07D233/48 ,  C07D49/34

CPC分类号： C07D233/48

摘要： The imidazoline 4-(3,4-dichlorophenyl)-2-(methylamino)-2imidazoline and non-toxic pharmaceutically acceptable acid addition salts thereof are useful as antihypertensive agents. Displacement of the methyl mercapto grouping from 2-methylthio-4(3,4-dichlorophenyl)-2-imidazoline with methylamine provides the imidazoline of the present invention.

摘要翻译： 咪唑啉4-（3,4-二氯苯基）-2-（甲基氨基）-2-咪唑啉及其无毒的药学上可接受的酸加成盐可用作抗高血压药。 甲基巯基从2-甲硫基-4-（3,4-二氯苯基）-2-咪唑啉与甲胺的置换提供了本发明的咪唑啉。

公开(公告)号：US3886278A

公开(公告)日：1975-05-27

申请号：US39045673

申请日：1973-08-22

申请人： MEAD JOHNSON & CO

发明人： GALLO DUANE GORDON

IPC分类号： C07C57/42 ,  C07D295/02 ,  C07D295/027 ,  A61K27/00

CPC分类号： C07D295/027 ,  C07C57/42 ,  Y10S514/859

摘要： The ammonium and amine salts of 3-methyl-5-phenyl-2-trans-4trans-pentadienoic acid and of the 2-lower alkyl-3-methyl-5phenyl-2-trans-4-trans-pentadienoic acids when applied locally to the skin where excess sebum production occurs have the capacity of reducing the sebum production and thereby alleviating conditions correlary to the excess production of sebum such as acne.

摘要翻译： 3-甲基-5-苯基-2-反式-4-反戊烯二酸和2-低级烷基-3-甲基-5-苯基-2-反式-4-反戊烯二酸的铵盐和胺盐 当局部施用于发生过量皮脂产生的皮肤时具有减少皮脂产生的能力，从而减轻与皮脂过量产生如痤疮相关的条件。

公开(公告)号：US3853949A

公开(公告)日：1974-12-10

申请号：US30094272

申请日：1972-10-26

申请人： MEAD JOHNSON & CO

发明人： COMER W ,  RAYBURN J ,  TEMPLE D

IPC分类号： C07C33/025 ,  C07C57/26 ,  C07C61/26 ,  C07C69/74

CPC分类号： C07C33/025 ,  C07C57/26

摘要： Dieneoic acid delta -methylene-1-cyclopentene-1-pentanoic acid is obtained by reacting cyclopentanone with one chemical equivalent of methylsulfinylmethide alkali metal salt in dimethyl sulfoxide. Lithium aluminum hydride reduction of the acid provides Epsilon -methylene-1-cyclopentene-1-pentanol. The acid, metal salts thereof, lower alkyl esters, and the alcohol are effective antifungal agents.

摘要翻译： 二烯酸δ-亚甲基-1-环戊烯-1-戊酸是通过环戊酮与一种化学当量的甲基亚磺酰基甲基碱金属盐在二甲亚砜中反应得到的。 氢化铝锂还原酸提供ε-亚甲基-1-环戊烯-1-戊醇。 其酸金属盐，低级烷基酯和醇是有效的抗真菌剂。

公开(公告)号：US3851648A

公开(公告)日：1974-12-03

申请号：US40561673

申请日：1973-10-11

申请人： MEAD JOHNSON & CO

发明人： BROOKE D

IPC分类号： C02F1/00 ,  A01M7/00 ,  A61F6/14 ,  A61J3/08 ,  A61K9/00 ,  A61K9/20 ,  A61K47/30 ,  A61M31/00 ,  A61M37/00 ,  B01J4/00 ,  B01J19/00 ,  A61M7/00

CPC分类号： A61J3/08 ,  A01M7/0092 ,  A61F6/14 ,  A61K9/0004 ,  A61K9/2072 ,  A61M31/002 ,  A61M37/00

摘要： A diffusible solid is released by diffusion into a fluid medium from a cavity within a container through an opening therein at a rate which is independent of the amount of solid present in the container. Zero-order release is effected by the shape of the cavity and the opening. The rate is related to the solubility and to the diffusion constant of the solid in the fluid medium. For a given substance, the rate of release is determined by cavity shape and dimensions of the diffusion opening. The device is adapted for use in both liquid and gaseous media and can be used for the zero-order release of drug substances into the system of a living organism, and for non-medical uses.

摘要翻译： 可扩散的固体通过与容器中存在的固体量无关的速率通过其中的开口从容器内的空腔扩散入流体介质而被释放。 零级释放由空腔和开口的形状来实现。 该速率与固体在流体介质中的溶解度和扩散常数有关。 对于给定的物质，释放速率由扩散开口的腔体形状和尺寸确定。 该装置适用于液体和气体介质，可用于药物物质零排放到生物体系统和非医疗用途中。

公开(公告)号：US3840522A

公开(公告)日：1974-10-08

申请号：US28034672

申请日：1972-08-14

申请人： MEAD JOHNSON & CO

发明人： COMER W ,  SCARBOROUGH P ,  LARSEN A ,  SCARBOROUGH H

IPC分类号： C07D225/06 ,  C07D41/00 ,  C07D99/04

CPC分类号： C07D225/06

摘要： 1. A COMPOUND SELECTED FROM THE GROUP CONSISTING OF COMPOUNDS OF THE FORMULA

3-R2,3-(R''-O2S-),5-R5,6-R6,6-R10,8-R8,9-R9-HEXAHYDRO-

(-N(-R)-(CH2)N-)(-R1)>C=N-CH(-Y)-(PHENYLENE)-(X)M

BENZAZOCINE

3-R2,3-(R''-O2S-),5-R5,6-R10,8-R8,9-R9-HEXAHYDROBENZAZOCINE

WHEREIN R2 AND R5 ARE EACH SELECTED FROM THE GROUP CONSISTING OF HYDROGEN AND LOWER ALKYL HAVING FROM 1 TO 4 CARBON ATOMS; R'' IS SELECTED FROM THE GROUP CONSISTING OF LOWER ALKYL HAVING UP TO 6 CARBON ATOMS, ARYL, AND ARALKYL EACH HAVING UP TO 12 CARBON ATOMS; R6 IS SELECTED FROM THE GROUP CONSISTING OF HYDROGEN, HYDROXY, CHLORO, AND BROMO; R8 AND R9 ARE SELECTED FROM THE GROUP CONSISTING OF HYDROGEN, HYDROXY, LOWER ALKYL HAVING UP TO 4 CARBON ATOMS, AND LOWER ALKOXY HAVING UP TO 4 CARBON ATOMS, AND R8 AND R9 TOGETHER FORM THE METHYLENEDIOXY GROUP; AND R10 IS SELECTED FROM THE GROUP CONSISTING OF HYDROGEN, ALKYL HAVING UP TO 8 CARBON ATOMS, AND ARYL HAVING UP TO 10 CARBON ATOMS.

公开(公告)号：US3809697A

公开(公告)日：1974-05-07

申请号：US18725771

申请日：1971-10-07

申请人： MEAD JOHNSON & CO

发明人： MARTIN T ,  COMER W

IPC分类号： C07D295/18 ,  A61K31/495 ,  C07D295/185 ,  C07D51/70

CPC分类号： C07D295/185 ,  A61K31/495

摘要： 1,4-BIS-ACYLIPERAZINES IN WHICH THE ACYL GROUP IS MERCAPTOACETYL OR A-SUBSTITUTED MERCAPTOACETYL ARE POTENT MUCOLYTIC AGENTS WHICH ARE NOT ONLY EFFECTIVE TOPICALLY BUT ALSO SYSTEMICALLY ON ORAL OR PARENTERAL ADMINISTRATION TO ANIMALS.

公开(公告)号：US3743746A

公开(公告)日：1973-07-03

申请号：US3743746D

申请日：1970-05-19

申请人： MEAD JOHNSON & CO

发明人： DUNGAN K ,  LISH P

IPC分类号： A61K31/00 ,  A61K27/00

CPC分类号： A61K31/00

摘要： ADMINISTRATION OF 1-(2-DIMETHYLAMINOETHYL)-1-PHENYLINDENE OR 1-(2-(METHYLAMINO)ETHYL)-1-PHENYLINDENE TO MAMMALS HAVING PEPTIC ULCER PRODUCES AN ANTIULCER EFFECT THEREIN. THE AFOREMENTIONED COMPOUNDS EMPLOYED IN THE PROCESS HAVE LITTLE DEMONSTRABLE ANTICHOLLINERGIC ACTIVITY AND PRODUCE THEIR ANTIULCER EFFECT BY A MECHANISM WHICH IS NON-ANTICHLOLINERGIC IN CHARACTER.

公开(公告)号：US3719671A

公开(公告)日：1973-03-06

申请号：US3719671D

申请日：1971-05-27

申请人： MEAD JOHNSON & CO

发明人： WU Y ,  LOBECK W

IPC分类号： C07D401/14 ,  C07D413/14 ,  C07D417/04 ,  C07D417/14 ,  C07D93/14

CPC分类号： C07D417/04 ,  C07D401/14 ,  C07D413/14 ,  C07D417/14 ,  Y10S514/869 ,  Y10S514/906 ,  Y10S514/96 ,  Y10S514/962

摘要： Novel 10-imidoylphenothiazines are prepared by reacting a phenothiazine which may have hydrogen, trifluoromethyl, methylthio, alkyl, alkoxy or halogen substituents in the 2 or 4 position with a carboxamide selected from the group consisting of amides and lactams in the presence of phosphorus oxychloride. Typical embodiments are 10-(2-(5-methyl-1pyrrolinyl))phenothiazine and 10-(2-(5,5-dimethyl-1pyrrolinyl))phenothiazine. The phenothiazine amidine products are useful as intestinal relaxant and antithromogenic agents.

摘要翻译： 通过在磷酰氯存在下使吩噻嗪，吩恶嗪或吖啶酮与吡咯烷酮反应获得选自吩噻嗪，吩恶嗪和吖啶的双吡咯啉衍生物的新型脒化合物。 吩噻嗪，吩恶嗪或吖啶也可以用2-氯-1-（1-吡咯啉-2-基）-2-吡咯啉烷基化，得到本发明的化合物。 双吡咯啉衍生物的典型实例是2-甲氧基-10- [5-甲基-1-（5-甲基-1-吡咯啉-2-基）-2-吡咯啉-2-基] - 异噻唑啉，10- [ 1-（1-吡咯啉-2-基）-2-吡咯啉-2-基]吩恶嗪和9,9-二甲基-10- [5-甲基-1-（5-甲基-1-吡咯啉-2-基 ）-2-吡咯啉-2-基]吖啶。 脒化合物可用作利尿剂，平滑肌松弛剂和抗血栓形成剂。

公开(公告)号：US3679702A

公开(公告)日：1972-07-25

申请号：US3679702D

申请日：1971-03-12

申请人： MEAD JOHNSON & CO

发明人： WU YAO HUA ,  RYAN RICHARD P JR

IPC分类号： C07D487/04 ,  C07D27/56

CPC分类号： C07D487/04

摘要： 1-(2-Amino- Alpha -(3-indolyl)phenethyl)-2-pyrrolidinone is a new synthetic compound having pharmacological value as a diuretic agent and as a chemical intermediate in the preparation of other diuretics and azo dyestuffs. This substance is prepared by basic hydrolysis of 2,3,5,6-tetrahydro-5-(indol-3-yl)-1H-pyrrolo(2,1b)(1,3) benzodiazepine.

摘要翻译： 1- [2-氨基-α-（3-吲哚基）苯乙基] -2-吡咯烷酮是具有药理学价值的新型合成化合物作为利尿剂，作为制备其它利尿剂和偶氮染料的化学中间体。 该物质通过2,3,5,6-四氢-5-（吲哚-3-基）-1H-吡咯并[2,1-b] [1,3]苯并二氮杂的碱性水解制备。

公开(公告)号：US3679692A

公开(公告)日：1972-07-25

申请号：US3679692D

申请日：1969-10-01

申请人： MEAD JOHNSON & CO

发明人： WU YAO HUA ,  LOBECK WALTER G

IPC分类号： C07D209/08 ,  C07D31/42

CPC分类号： C07D209/08

摘要： This invention relates to a series of 1-iminomethylindolines which are analeptic agents capable of counteracting central nervous system depressant effects of pentobarbital and chloral hydrate. They also exhibit analgesic effects. This invention also relates to a process for the preparation of 1iminomethylindolines which comprises reaction of an indoline with carboxamides selected from the group consisting of amides, lactams, symmetrical or unsymmetrical ureas and hydrazides. Typical examples of 1-iminomethylindoline derivatives are 5acetyl-1-(2-(1-pyrrolinyl)) indoline and 1-(2-(5,5-dimethyl-1pyrrolinyl)) indoline.

摘要翻译： 本发明涉及一系列能够抵抗戊巴比妥和水合氯醛的中枢神经系统抑制作用的消炎药的1-亚氨基甲基吲哚啉。 他们也表现出止痛作用。 本发明还涉及制备1-亚氨基甲基吲哚啉的方法，其包括二氢吲哚与选自酰胺，内酰胺，对称或不对称的脲和酰肼的羧酰胺的反应。 1-亚氨基甲基二氢吲哚衍生物的典型实例是5-乙酰基-1- [2-（1-吡咯啉基）]二氢吲哚和1- [2-（5,5-二甲基-1-吡咯啉基）]二氢吲哚。