公开(公告)号：US4044017A

公开(公告)日：1977-08-23

申请号：US740894

申请日：1976-11-11

申请人： Cedric Herbert Hassall ,  William Henry Johnson ,  Antonin Krohn ,  Carey Ernest Smithen ,  William Anthony Thomas

发明人： Cedric Herbert Hassall ,  William Henry Johnson ,  Antonin Krohn ,  Carey Ernest Smithen ,  William Anthony Thomas

IPC分类号： A61K38/00 ,  C07D213/50 ,  C07D243/24 ,  C07D249/08 ,  C07K5/06 ,  C07K5/065 ,  C07K5/068 ,  C07K5/072 ,  C07K5/078 ,  C07D249/06

CPC分类号： C07K5/06191 ,  C07D213/50 ,  C07D243/24 ,  C07D249/08 ,  C07K5/06026 ,  C07K5/06034 ,  C07K5/06043 ,  C07K5/06078 ,  C07K5/06086 ,  C07K5/06095 ,  C07K5/06104 ,  C07K5/06165 ,  A61K38/00 ,  Y10S514/906

摘要： This invention is directed toward pharmacologically active compounds of the formula ##STR1## wherein A represents a nitrogen atom which may be substituted by a methyl, cyclopropylmethyl, di(C.sub.1-4 alkyl)aminoethyl, methoxymethyl or hydroxyethyl group and B represents a carbonyl group or A and B together represent a grouping of the formula ##STR2## in which R.sup.a represents a hydrogen atom or a lower alkyl or hydroxymethyl group and X represents a nitrogen atom or C-R.sup.b wherein R.sup.b represents a hydrogen atom or a lower alkyl or hydroxymethyl group; R represents a halogen atom or a nitro or trifluoromethyl group; R.sup.1 represents a hydrogen atom or a lower alkyl group; R.sup.2 represents an acyl group derived from a naturally occurring amino acid (all such groups which contain an asymmetric carbon atom having the L- or D,L-configuration) and R.sup.3 represents a phenyl, halophenyl or 2-pyridyl groupAnd acid addition salts thereof.Also provided are methods for their preparation and intermediates thereof, These compounds exhibit activity as anticonvulsants, muscle relaxants and sedatives.

摘要翻译： 本发明涉及下式的药理学活性化合物，其中A表示可被甲基，环丙基甲基，二（C 1-4烷基）氨基乙基，甲氧基甲基或羟乙基取代的氮原子，B表示羰基或A 和B一起表示其中R a表示氢原子或低级烷基或羟甲基并且X表示氮原子的式“IMAGE”或其中R b表示氢原子或低级烷基或羟甲基的C-R b的基团; R表示卤素原子或硝基或三氟甲基; R1表示氢原子或低级烷基; R 2表示衍生自天然存在的氨基酸的酰基（所有这些基团含有具有L或D，L构型的不对称碳原子），R 3表示苯基，卤代苯基或2-吡啶基。其酸加成盐 。

公开(公告)号：US4009175A

公开(公告)日：1977-02-22

申请号：US666902

申请日：1976-03-15

申请人： Jackson B. Hester, Jr.

发明人： Jackson B. Hester, Jr.

IPC分类号： A61K31/55 ,  A61P25/20 ,  A61P25/24 ,  A61P25/26 ,  C07D213/50 ,  C07D487/04

CPC分类号： C07D487/04 ,  C07D213/50 ,  Y10S514/906

摘要： Compounds of the formula: ##STR1## wherein R'o and R"o are hydrogen or alkyl of 1 to 3 carbon atoms, inclusive; R.sub.1 is hydrogen, fluoro, chloro, bromo, nitro, trifluoromethyl, or alkylthio in which the alkyl moiety is of 1 to 3 carbon atoms, inclusive; R.sub.2 is phenyl, o-chlorophenyl, 0-fluorophenyl, 2,6-difluorophenyl and 2-pyridyl are prepared by multistep reactions from compounds of formula I: ##STR2## wherein R.sub.1 and R.sub.2 are defined as above and X is chlorine or bromine.Compounds of formula III, intermediates in the preparation thereof, Schiff's bases of compounds IIIA (III in which R'o and R"o are hydrogen), and the pharmacologically acceptable acid addition salts are useful in birds and mammals, including man, as sedatives, antianxiety, antidepressant, anticonvulsive, and muscular relaxing agents.

摘要翻译： 下式的化合物：其中R'o和R'o是氢或1至3个碳原子的烷基（包括端值）; R1是烷基部分为1-3个碳原子的氢，氟，氯，溴，硝基，三氟甲基或烷硫基; R2是苯基，邻氯苯基，O-氟苯基，2,6-二氟苯基和2-吡啶基，其通过式I化合物的多步反应制备：其中R 1和R 2如上定义，X​​是氯或溴 。

公开(公告)号：US4001215A

公开(公告)日：1977-01-04

申请号：US666512

申请日：1976-03-12

申请人： Thomas J. Dietsche

发明人： Thomas J. Dietsche

IPC分类号： C07D213/50 ,  C07D245/02

CPC分类号： C07D213/50 ,  C07D245/02

摘要： The title compound is readily prepared in good yield by the reaction of acetylacetone with ammonia in methanol. It has fungicidal and insecticidal properties and, by reason of the number and variety of functional groups it contains, should be useful as an intermediate.

公开(公告)号：US4000143A

公开(公告)日：1976-12-28

申请号：US620907

申请日：1975-10-08

申请人： Stanley J. Dykstra ,  Joseph L. Minielli

发明人： Stanley J. Dykstra ,  Joseph L. Minielli

IPC分类号： C07D211/22 ,  C07D211/26 ,  C07D213/26 ,  C07D213/30 ,  C07D213/38 ,  C07D213/40 ,  C07D213/50 ,  C07D211/18

CPC分类号： C07D213/30 ,  C07D211/22 ,  C07D211/26 ,  C07D213/26 ,  C07D213/38 ,  C07D213/40 ,  C07D213/50 ,  Y10S514/821

摘要： The compounds are of the heterocyclic class of 2-phenethylpiperidines having an amido substituent in the ortho position of the phenethyl moiety. Substituents in the ortho position include formamido, benzamido, cinnamamido, 2-thiophenecarboxamido, alkanesulfonamido and alkanoylamido. They are useful as antiarrhythmic and/or antiserotonin agents. The novel compounds are prepared by reaction of appropriately substituted o-aminophenethylpiperidines and the carbonyl or sulfonyl halides or anhydrides. Typical embodiments of this invention are 4-methoxy-2'-[2-(1-methyl-2-piperidyl)ethyl]benzanilide and 2'-[2-(1-methyl-2-piperidyl)ethyl]cinnamanilide.

公开(公告)号：US3969363A

公开(公告)日：1976-07-13

申请号：US531325

申请日：1974-12-10

申请人： Thomas Raabe ,  Otto Grawinger ,  Josef Scholtholt ,  Rolf-Eberhard Nitz ,  Eckhard Schraven

发明人： Thomas Raabe ,  Otto Grawinger ,  Josef Scholtholt ,  Rolf-Eberhard Nitz ,  Eckhard Schraven

IPC分类号： C07D213/38 ,  C07D213/50 ,  C07D213/85 ,  C07D303/24 ,  C07D413/06 ,  C07D213/72

CPC分类号： C07D303/24 ,  C07D213/38 ,  C07D213/50 ,  C07D213/85

摘要： The present invention relates to new pharmacologically valuable derivatives of 1-phenoxy-3-amino-propan-2-ol having the formula ##EQU1## and the aldehyde condensation products and acid addition salts thereof wherein X is selected from the group consisting of ##EQU2## wherein the phenyl ring I may have attached to it up to three similar or different substituents selected from the group consisting of alkyl, alkenyl, alkinyl, cycloalkyl, cycloalkenyl, alkoxy, alkenyloxy, alkinyloxy, benzyloxy, phenyl, halogen and --NR.sub.1 R.sub.2, wherein R.sub.1 is selected from alkyl and acyl, and R.sub.2 is selected from hydrogen and alkyl and n is 1, 2 or 3; and to the production thereof by a method selected from (A) reacting 1-phenoxy-3-amino-propan-2-ol having the formula ##EQU3## with a compound having the formula Y-X, wherein X has the above defined meaning and Y is selected from halogen, --OH, --OK or --ONa; (B) reacting a compound of the formula ##EQU4## with a compound of the formula H.sub.2 N--X, wherein X has the above-defined meaning and Z is selected from ##EQU5## and ##EQU6## (C) reacting a phenol ##EQU7## with Z--CH.sub.2 --NH--X, wherein X and Z have the meaning defined above.

摘要翻译： 本发明涉及具有式-O-CH2-CH-CH2-NH-X | OH的1-苯氧基-3-氨基 - 丙-2-醇的新药理学上有价值的衍生物及其醛缩合产物及其酸加成盐 其中X选自-C = CH-C和| PARALLEL CH3O -CH-CH2-CH || CH3OH，其中苯环I可以连接至最多三个相似或不同的取代基，所述取代基选自 烷基，烯基，炔基，环烷基，环烯基，烷氧基，烯氧基，链烯氧基，苄氧基，苯基，卤素和-NR1R2，其中R1选自烷基和酰基，R2选自氢和烷基，n为1,2或 3; 并通过选自（A）使具有式-O-CH 2 -CH-CH 2 -NH 2 | OH的1-苯氧基-3-氨基 - 丙-2-醇与具有式YX的化合物反应的方法制备， 其中X具有上述含义，Y选自卤素，-OH，-OK或-ONa; （B）使式-O-CH2-Z的化合物与式H2N-X的化合物反应，其中X具有上述定义，Z选自-CH-CH 2 ANGLE O和-CH 2 -CH 2 - 卤素; | OH（C）使苯酚-OH与Z-CH2-NH-X反应，其中X和Z具有上述定义。

公开(公告)号：US3917622A

公开(公告)日：1975-11-04

申请号：US45530674

申请日：1974-03-27

申请人： BAYER AG

发明人： MEYER HORST ,  BOSSERT FRIEDRICH ,  VATER WULF ,  STOEPEL KURT

IPC分类号： C07D401/04 ,  C07D405/04 ,  C07D409/04 ,  C07D213/50

CPC分类号： C07D401/04 ,  C07D405/04 ,  C07D409/04 ,  Y10S514/929

摘要： 2-Amino-1,4-dihydropyridines bearing a carbonyl function in the 5-position and being optionally substituted by lower alkyl or phenyl in the 6-position, and the corresponding 2-amino1,4,5,6,7,8-hexahydro-5-oxoquinolines, which derivatives are further substituted by a carbonyl group in the 3-position and optionally substituted in the 4-position by lower alkyl, phenyl, substituted phenyl or a heterocyclic group are antihypertensive agents and coronary vessel dilators. The compounds, of which 2amino-6-methyl-4-(3-nitrophenyl)-1,4-dihydropyridine-3,5dicarboxylic acid 3,5-diethyl ester is a representative embodiment, are prepared through condensation of an ylideneacetoacetic acid ester and an amidine.

公开(公告)号：US3910933A

公开(公告)日：1975-10-07

申请号：US40814773

申请日：1973-10-19

申请人： SMITHKLINE CORP

发明人： KAISER CARL ,  WARDELL JR JOE R

IPC分类号： A61K31/445 ,  C07D211/02 ,  C07D211/22 ,  C07D213/30 ,  C07D213/50 ,  C07D211/26

CPC分类号： A61K31/445 ,  C07D211/02 ,  C07D211/22 ,  C07D213/50 ,  Y10S514/825 ,  Y10S514/96

摘要： 3-Substituted-3-hydroxyphenyl-2-piperidylcarbinols are prepared. These compounds are Beta -adrenergic stimulants and are useful in particular as bronchodilators.

摘要翻译： 制备3-取代的3-羟基苯基-2-哌啶基甲醇。 这些化合物是β-肾上腺素能兴奋剂，特别可用作支气管扩张剂。

公开(公告)号：US3781444A

公开(公告)日：1973-12-25

申请号：US3781444D

申请日：1971-11-12

申请人： REYNOLDS TOBACCO CO R

发明人： HAEFELE L ,  EZZELL B ,  FLUCK E

IPC分类号： C07D213/50 ,  A61K27/00

CPC分类号： C07D213/50

摘要： BENZYL-SUBSTITUTED CYCLOOCTANONE COMPOUNDS WHICH EXHIBIT HYPOCHOLESTEROLEMIC PROPERTIES.

公开(公告)号：US3776916A

公开(公告)日：1973-12-04

申请号：US3776916D

申请日：1972-06-07

申请人： MONSANTO CO

发明人： PHILLIPS W

IPC分类号： A01N35/04 ,  A01N43/48 ,  C07D213/20 ,  C07D213/50 ,  C07D213/61 ,  C07D213/63 ,  C07D213/84 ,  C07D31/46

CPC分类号： C07D213/84 ,  A01N35/04 ,  A01N43/48 ,  C07D213/20 ,  C07D213/50 ,  C07D213/61 ,  C07D213/63

摘要： PYRIDINIUM, PYRIDAZINIUM, PYRIMIDINIUM, AND PYRAZINIUM HALIDES RESPECTIVELY HAVING AN N-(PHENACYL) SUBSTITUENT AND THE CORRESPONDING YLIDS OBTAINED THEREFROM BY ALKALINE TREATMENT WHICH COMPOUNDS ARE USEFURL AS HERBICIDES AND/OR INSECTICIDES.

公开(公告)号：US3763148A

公开(公告)日：1973-10-02

申请号：US3763148D

申请日：1972-07-31

申请人： MARKOVAC A ,  MONTAGNE M ,  ASH A ,  BLUMBERGS P

发明人： MARKOVAC A ,  LA MONTAGNE M ,  ASH A ,  BLUMBERGS P

IPC分类号： C07C45/63 ,  C07C59/88 ,  C07D213/20 ,  C07D213/38 ,  C07D213/50 ,  C07D213/79 ,  C07D31/36

CPC分类号： C07D213/79 ,  C07C45/63 ,  C07C59/88 ,  C07D213/20 ,  C07D213/38 ,  C07D213/50 ,  Y10S514/895 ,  C07C49/80

摘要： A SERIES OF TRIFLUOROMETHYL SUBSTITUTED-2,6-DIPHENYL-4PYRIDYLCARBINOLAMINES IS HEREIN DISCLOSED WHICH HAS VALUE IN TREATMENT OF PLASMODIAL INFECTIONS. THE COMPOUNDS HAVE SUBSTITUTED PHENYL GROUPS AT POSITIONS 2- AND 6- ON THE PYRIDINE MOIETY, WITH THE ELECTRONEGATIVE SUBSTITUENTS (THE SAME, OR DIFFERENT) PRESENT ON THE PHENYL NUCLEI AT LEAST ONE OF WHICH IS TRIFLUOROMETHYL. THE SYNTHESES OF SUCH SERIES IS DESCRIBED, TOGETHER WITH A METHOD FOR SEPARATION OF RACEMATES OF A REPRESENTATIVE 4-PYRIYLCAR BINOLAMINE TYPE.