公开(公告)号：US3553209A

公开(公告)日：1971-01-05

申请号：US3553209D

申请日：1968-12-16

申请人： PARKE DAVIS & CO

发明人： ITALIEN YVON J L ,  NORDIN IVAN C

IPC分类号： C07D231/16 ,  C07D231/38 ,  C07D487/04 ,  C07D53/02

CPC分类号： C07D231/38 ,  C07D231/16 ,  C07D487/04

摘要： 3 - METHYL-8-(2-THIENYL)PYRAZOLO(4,3-E)(1,4)DIAZEPIN5(4H)-ONE COMPOUNDS, 7-OXIDE DERIVATIVES THEREOF, AND THEIR SALTS, SUBSTITUTED IN THE 1-POSITION BY METHYL OR ETHYL AND OPTIONALLY IN THE 4-POSITION BY METHYL; AND THEIR PRODUCTION BY (A) REACTING A 4-AMINO-3-METHYL-5(2-THENOYL)PYRAZOLE WITH A LOWER ALKYL ESTER OF GLYCINE OR A SALT THEREOF, (B) REACTING A 4-(2-HALOACETAMIDO)-3METHYL-5-(2-THENOYL)PYRAZOLE OR A SALT THEREOF WITH AMMONIA, (C) REACTING A 4-(2-AMINOACETAMIDO)-3-METHYL5-(2-THENOYL)PYRAZOLE SALT WITH A BASE, (D) REACTING A 4-(2-(HYDROXYLAMINO)ACETAMIDO) - 3 - METHYL-5-(2-THENOYL)PYRAZOLE WITH A STRONG ACID, (E) REACTING ONE OF THE 3-METHYL - 8 - (2-THIENYL)PYRAZOLO(4,3-E)(1,4)DIAZEPIN-5 (1H)-ONE COMPOUNDS WITH AN OXIDIZING AGENT, AND (F) REACTING ONE OF THE 4-UNSUBSTITUTED 3-METHYL-8-(2-THIENYL)PYRAZOLO(4,3-E)(1,4)DIAZEPIN-5(1H) ONES OR THE 7-OXIDE DERIVATIVES THEREOF WITH A METHYLATING AGENT IN THE PRESENCE OF A BASE. THE COMPOUNDS OF THE INVENTION ARE USEFUL AS ANTICONVULSANT AND ANTI-ANXIETY AGENTS.

公开(公告)号：US3557103A

公开(公告)日：1971-01-19

申请号：US3557103D

申请日：1968-07-18

申请人： PARKE DAVIS & CO

发明人： NORDIN IVAN C

IPC分类号： C07D265/36 ,  C07D87/48

CPC分类号： C07D265/36

摘要： NOVEL BENZOXAZINONE FREE BASE (I) AND ACID ADDITION SALT COMPOUNDS

2-PHENYL,4-(A=N-(CH2)N-)-3,4-DIHYDRO-2H-1,4-BENZOXAZIN-3-

ONE

ARE PROVIDED BY CONDENSING 2-PHENYL-2H-1,4-BENZOXAZIN3(4H)-ONE WITH THE APPROPRIATE AMINOALKYL SIDE CHAIN IN EITHER ONE OR TWO STEPS WHERE B IS 3, 4 OR 5 AND -N=A IS A DIISOPROPYLAMINO, 2,5-DIMETHYL-1-PYRROLIDINYL OR 2,6DIMETHYLPIPERIDINO GROUP. THE PRODUCTS HAVE PHARMACOLOGICAL PROPERTIES AND ARE USEFUL ANTI-ARRHYTHMIC AGENTS.

公开(公告)号：US3553210A

公开(公告)日：1971-01-05

申请号：US3553210D

申请日：1968-12-16

申请人： PARKE DAVIS & CO

发明人： NORDIN IVAN C

IPC分类号： C07D231/16 ,  C07D231/38 ,  C07D231/40 ,  C07D231/42 ,  C07D487/04 ,  C07D53/02

CPC分类号： C07D231/38 ,  C07D231/16 ,  C07D231/40 ,  C07D231/42 ,  C07D487/04

摘要： 3-METHYL-8-PHENYLPYRAZOLO(4,3-E)(1,4)DIAZEPIN-5(1H)ONE, 7-OXIDE COMPOUNDS, SUBSTITUTED IN THE 1-POSITION BY METHYL OR ETHYL AND OPTIONALLY IN THE 4-POSITION BY METHYL; SALTS THEREOF; AND THEIR PRODUCTION BY (A) REACTING A 5 - BENZOYL-4-(HYDROXYAMINO)ACETAMIDO-3METHYLPYRAZOLE WITH A STRONG ACID; (B) REACTING A 3-METHYL-8-PHENYLPYRAZOLO(4,3-E)(1,4)DIAZEPIN-5(1H)ONE WITH AN OXIDIZING AGENT, AND (C) REACTING ONE OF THE 4-UNSUBSTITUTED 3-METHYL-8-PHENYLPYRAZOLO(4,3-E)(1,4) DIAZEPIN-5(1H)-ONE, 7-OXIDES WITH A METHYLATING AGENT IN THE PRESENCE OF A BASE. THE COMPOUNDS OF THE INVENTION ARE USEFUL AS ANTICONVULSANT AND ANTIANXIETY AGENTS.

公开(公告)号：US3553207A

公开(公告)日：1971-01-05

申请号：US3553207D

申请日：1968-12-16

申请人： PARKE DAVIS & CO

发明人： NORDIN IVAN C

IPC分类号： C07D231/16 ,  C07D231/38 ,  C07D231/42 ,  C07D487/04 ,  C07D53/02

CPC分类号： C07D231/38 ,  C07D231/16 ,  C07D231/42 ,  C07D487/04

摘要： 6-HYDROXY-AND 6-ACETOXY - 3 - METHYL - 8 - PHENYLPYRAZOLO(4,3-E)-(1,4)DIAZEPIN - 5(1H) - ONE COMPOUNDS SUBSTITUTED IN THE 1-POSITION BY METHYL OR ETHYL AND OPTIONALLY IN THE 4 POSITION BY METHYL; SALTS THEREOF; AND THEIR PRODUCTION BY (A) REACTING A 3-METHYL-8-PHENYLPYRAZOLODIAZEPINONE, 7-OXIDE COMPOUND WITH ACETIC ANHYDRIDE TO PRODUCE ONE OF THE 6-ACETOXY COMPOUNDS AND (B) HYDROLYZING ONE OF THE 6-ACETOXY COMPOUNDS TO PRODUCE ONE OF THE CORRESPONDING 6-HYDROXY COMPOUNDS. THE COMPOUNDS OF THE INVENTION ARE USEFUL AS ANTICONVULSANT AND ANTI-ANXIETY AGENTS.

公开(公告)号：US3886143A

公开(公告)日：1975-05-27

申请号：US43481774

申请日：1974-01-21

申请人： PARKE DAVIS & CO

发明人： NORDIN IVAN C

IPC分类号： C07D231/40 ,  C07D498/14 ,  C07D99/02

CPC分类号： C07D231/40

摘要： Oxazolo(3,2-d)pyrazolo(4,3-f)(1,4)diazepin-6(7H)-ones and methods for their preparation are disclosed. The compounds can be prepared by either of the following procedures: (a) Reacting 4(o-fluorophenyl)-6,8-dihydro-1,3,8-trimethylpyrazolo(3,4e)(1,4)diazepin -7(1H)-one with an alkylene oxide; or (b) cyclizing the appropriately substituted 4-(o-fluorobenzoyl)-1,3dimethyl-5-(N-methyl-(2 -hydroxyalkylamino)acetamido)pyrazole via heat or an acid catalyst. The compounds are pharmacological agents, especially anticonvulsants.

摘要翻译： 公开了唑并[3,2-d]吡唑并[4,3-f] [1,4]二氮杂-6（7H） - 酮及其制备方法。 化合物可以通过以下任一方法制备：（a）使4-（邻氟苯基）-6,8-二氢-1,3,8-三甲基吡唑并[3,4-e] [1,4]二氮杂 环庚烯-7（1H） - 酮与烯化氧; 或（b）通过加热或酸催化剂使适当取代的4-（邻氟苯甲酰基）-1,3-二甲基-5-（N-甲基 - [2-羟基烷基氨基]乙酰氨基）吡唑环化。 这些化合物是药理剂，特别是抗惊厥药。

公开(公告)号：US3879395A

公开(公告)日：1975-04-22

申请号：US40855673

申请日：1973-10-23

申请人： PARKE DAVIS & CO

发明人： NORDIN IVAN C

IPC分类号： C07D295/13 ,  C07D51/70

CPC分类号： C07D295/13

摘要： 3-(4-(O-(Propylthio)phenyl)-1-piperazinylalkylamino)-2cycloalken-1-ones, and acid-addition salts, thereof, are pharmacological agents, especially central nervous system depressants of the type known as major tranquilizing agents. They exhibit cerebral depressant activity and suppress conditioned avoidance behavior. Said compounds can be produced by condensation of a 4-(o-(propylthio)phenyl)-1piperazinylalkylamine with the appropriate 1,3-cycloalkanedione.

摘要翻译： 3- [4- [O-（丙硫基）苯基] -1-哌嗪基烷基氨基] -2-环烯酮-1-酮及其酸加成盐是药理学剂，特别是已知为主要的中枢神经系统抑制剂 镇静剂。 他们表现出抑郁活动，抑制条件回避行为。 所述化合物可以通过将4- [O-（丙硫基）苯基] -1-哌嗪基烷基胺与适当的1,3-环烷二酮缩合而制备。

公开(公告)号：US3700657A

公开(公告)日：1972-10-24

申请号：US3700657D

申请日：1971-05-18

申请人： PARKE DAVIS & CO

发明人： NORDIN IVAN C

IPC分类号： C07D487/04 ,  C07D53/02

CPC分类号： C07D487/04

摘要： 3 - METHYL - 4,6,7,8 - TETRAHYDROPYRAZOLO(4,3-E)(1,4)DIAZEPIN-5(1H)-ONE, SUBSTITUTED IN THE 1-POSITION BY LOWER ALKYL AND OPTIONALLY IN THE 4- AND 7-POSITIONS BY METHYL; SALTS THEREOF; AND THEIR PRODUCTION BY CATALYTICALLY HYDROGENATING A DIHYDROPYAZOLODIAZEPINONE, OR BY REACTING ONE OF THE 7-UNSUBSTITUTERD TETRAHYDROPYRAZOLODIAZEPINONES WITH A METHYLATING AGENT. THE COMPOUNDS OF THE INVENTION ARE USEFUL AS ANTICONVULSANT AGENTS.

公开(公告)号：US3886144A

公开(公告)日：1975-05-27

申请号：US43476274

申请日：1974-01-21

申请人： PARKE DAVIS & CO

发明人： NORDIN IVAN C ,  DEWALD HORACE A

IPC分类号： C07D231/16 ,  C07D231/38 ,  C07D231/40 ,  C07D487/04 ,  C07D498/14 ,  C07D99/02

CPC分类号： C07D231/38 ,  C07D231/16 ,  C07D231/40 ,  C07D487/04

摘要： Oxazolo(and oxazino)(3,2-d)pyrazolo(3,4-f)(1,4)-diazepin-5(6H)ones and methods for the preparation are disclosed. The compounds can be prepared by one or more of the following procedures: Reaching the appropriately substituted pyrazolodiazepinone with an alkylene oxide; cyclizing the appropriately substituted 5aroyl-4-(2-(hydroxyalkylamino)acetamido)pyrazole via heat or an acid catalyst; reacting the appropriately substituted Schiff base of a pyrazole and/or oxazolidine of a pyrazole with a haloacylhalide in the presence of a base; reacting the appropriately substituted oxazolopyrazolodiazepinone or oxazinopyrazolodiazepinone with an alkylating agent in the presence of a base. The compounds are pharmacological agents, especially anticonvulsants.

摘要翻译： [3,2-d]吡唑并[3,4-f] [1,4] - 二氮杂-5（6H） - 酮及其制备方法。 化合物可以通过以下一种或多种方法制备：用烯化氧将适当取代的吡唑并噻吩酮 通过加热或酸催化剂使适当取代的5-芳酰基-4- [2-（羟基烷基氨基）乙酰氨基]吡唑环化; 使吡唑的适当取代的席夫碱和/或吡唑的恶唑烷与卤代酰卤在碱的存在下反应; 在碱的存在下，使适当取代的恶唑基四唑并噻吩酮或恶嗪基吡唑并氮杂酮与烷基化剂反应。 这些化合物是药理剂，特别是抗惊厥药。

公开(公告)号：US3562330A

公开(公告)日：1971-02-09

申请号：US3562330D

申请日：1968-07-18

申请人： PARKE DAVIS & CO

发明人： NORDIN IVAN C

IPC分类号： C07C93/06

CPC分类号： C07C217/64 ,  Y10S514/821

摘要： THE NOVEL AMINE COMPOUNDS, SPECIFICALLY 2-PHENOXY-4PHENYLBUTYLAMINE, 2-PHENOXY-5-PHENYLPENTYLAMINE AND THEIR ACID ADDITION SALTS, ARE PROVIDED BY CHEMICALLY REDUCING 2-PHENOXYPHENYLAMIDES (II):

PHENYL-(CH2)N-CH(-O-C6H5)-CO-NH2

WHERE N IS 2 OR 3. THE PRODUCTS HAVE PHARMACOLOGICAL PROPERTIES AND ARE USEFUL ANTIARRHYTHMIC AGENTS.

公开(公告)号：US3446811A

公开(公告)日：1969-05-27

申请号：US3446811D

申请日：1965-04-23

申请人： PARKE DAVIS & CO

发明人： NORDIN IVAN C ,  PARCELL ROBERT F

IPC分类号： C07D295/13 ,  C07D29/12 ,  C07C103/30

CPC分类号： C07D295/13 ,  Y10S514/821