专利快速检索-快速检索全球专利，免费商用专利数据库-IPRDB

1. 发明授权

US3853881A Dibenzo {8 b,f{9 -s-triazolo {8 4,3-d{9 {0 {8 1,4{9 {0 thiazepines-3-ones and dioxo derivatives thereof 失效
标题翻译： DIBENZO {8 B，F {9-S-TRIAZOLO {8,43-D {9 {0} {1,4 {9 {其中的三氮杂萘及其衍生物
公开(公告)号：US3853881A
公开(公告)日：1974-12-10
申请号：US38627973
申请日：1973-08-07
申请人： UPJOHN CO
发明人： SZMUSZKOVICZ J
IPC分类号： C07D487/04 , C07D513/04 , C07D99/10
CPC分类号： C07D487/04 , C07D513/04
摘要： Compounds of the formula IV:

wherein X is selected from the group consisting of sulfur and

WHEREIN R1 is selected from the group consisting of hydrogen, alkyl of one to three carbon atoms, inclusive;

IN WHICH N IS 2 OR 3, R7 and R8 are hydrogen or alkyl as defined above, or together

IS PYRROLIDINO, PIPERIDINO OR N-methylpiperazino; wherein R3 and R4 are selected from the group consisting of hydrogen, fluoro, chloro, bromo, or alkyl, defined as above, and alkoxy of one to three carbon atoms, inclusive, are prepared by reacting a thio compound of formula I:

wherein R3 and R4 are defined as above, in sequence: 1. WITH AN ALKYLCARBAZATE; AND THE RESULTING PRODUCT II 2. with an alkylating agent of the formula R1''Cl in which R1'' is alkyl as defined above,

AS DEFINED ABOVE IN THE PRESENCE OF A STRONG BASE; TO OBTAIN THE COMPOUND VI (with X'' is sulfur) as defined above. If X is

D R A W I N G
IS DESIRED THE COMPOUND II is oxidized e.g. m-perchlorobenzoic acid to give compound III or compound V may be oxidized to give a compound IV with R'' as substituent. Compounds of formula II, III, IV, and V can be presented in one formula as compound VI which including pharmacologically acceptable acid addition salts thereof has sedative and antidepressant activity and can be used in mammals.
摘要翻译：式IV化合物：

2. 发明授权

US3818003A Tricyclic benzodiazepines 失效
标题翻译：三氯苯甲酸
公开(公告)号：US3818003A
公开(公告)日：1974-06-18
申请号：US21511872
申请日：1972-01-03
申请人： UPJOHN CO
发明人： SZMUSZKOVICZ J
IPC分类号： C07D243/22 , A23K1/16 , A61K31/55 , A61K31/551 , A61P25/00 , A61P25/08 , A61P25/20 , C07D243/16 , C07D243/18 , C07D487/04 , C07D57/34
CPC分类号： C07D487/04
摘要： Novel 7-substituted-3,5-dihydro-as-triazino(4,3-a)(1,4)benzodiazepin-2(1H)-ones, 7-substituted-3,5-dihydro-astriazino(4,3-a)(1,4)benzodiazepine-2(1H) -thiones, the 6-oxide derivatives thereof, the intermediate 5-substituted-2,3-dihydro2-thioxo-1H-1,4-benzodiazepine-1-acetic acid alkyl esters, pharmacologically acceptable acid addition salts thereof, and processes for the production thereof. The compounds of this invention and the pharmacologically acceptable acid addition salts thereof are central nervous system depressants which are useful as sedatives, hypnotics, tranquilizers, muscle relaxants and anticonvulsants. They are also useful as feed additives for increasing growth rate and feed efficiency of livestock and poultry, milk production in mammals and egg production in birds.
摘要翻译：新的7-取代-3,5-二氢 - 三嗪并[4,3-a] - [1,4]苯并二氮杂-2（1H） - ，7-取代-3,5-二氢 - 4,3-a] [1,4]苯并二氮杂-2（1H） - 噻喃，其6-氧化物衍生物，中间体5-取代-2,3-二氢-2-硫代-1H-1,4-苯并二氮杂 -1-乙酸烷基酯，其药理学上可接受的酸加成盐及其制备方法。本发明化合物及其药理学上可接受的酸加成盐是可用作镇静剂，安眠药，镇静剂，肌肉松弛剂和抗惊厥药的中枢神经系统抑制剂。它们也可用作饲料添加剂，用于提高家畜和家禽的生长速度和饲料效率，哺乳动物产奶量和鸡蛋生产量。

3. 发明授权

US3856802A 1,6-DISUBSTITUTED-4H-5-{8 4,3-a{9 BENZODIAZEPINES 失效
标题翻译： 1,6-二异丁基-4H-5- {8,4,3-a {9 BENZODIAZEPINES
公开(公告)号：US3856802A
公开(公告)日：1974-12-24
申请号：US38066673
申请日：1973-07-19
申请人： UPJOHN CO
发明人： SZMUSZKOVICZ J
IPC分类号： C07D487/04 , C07D57/02 , C07D99/04 , C07D99/06
CPC分类号： C07D487/04 , Y10S514/906
摘要： 1,6-Disubstituted-4H-s-triazolo(4,3-a)(1,4)benzodiazepines of the formula II:

wherein R is an aromatic heterocyclic ring compound moiety selected from 2-, 3-, and 4-pyridyl, 2-thienyl, and 2-furyl; wherein R1 is selected from the group consisting of hydrogen and alkyl of one to three carbon atoms, inclusive; wherein R2, R3, R4, and R5 are selected from the group consisting of hydrogen, halogen, nitro, trifluoromethyl, and alkylthio in which alkyl is defined as above, are produced by condensing a 5-phenyl-1,3dihydro-2H-1,4-benzodiazepin-2-thione of the formula (I):

wherein R1, R2, R3, R4, and R5 are defined as above, with a hydrazine of the formula III:

in which R is defined as above. The new products of formula II including their pharmacologically acceptable acid addition salts and the N-oxides (in position 5) of II and the said salts are useful as sedatives, hypnotics, anticonvulsants, tranquilizers, and muscle relaxants in mammals and birds.
摘要翻译：式II的1,6-二取代-4H-哒嗪并[4,3-a] [1,4]苯并二氮杂：

4. 发明授权

US3714186A 7-(1-pyrrolidinyl)-endo-7-norcaranol and its method of preparation 失效
标题翻译： 7-（1-吡咯烷基）-ENDO-7-壬醇及其制备方法
公开(公告)号：US3714186A
公开(公告)日：1973-01-30
申请号：US3714186D
申请日：1971-06-02
申请人： UPJOHN CO
发明人： SZMUSZKOVICZ J , CERDA E
IPC分类号： C07D295/096 , C07D27/02
CPC分类号： C07D295/096
摘要： A process for the preparation of endo-7-norcaranol and intermediate compounds prepared by said process.
摘要翻译：一种制备通过所述方法制备的7-内啡诺内酯和中间体化合物的方法。

5. 发明授权

US3853904A DIBENZA-{8 b,f{9 -S-TRIAZOLO-{8 4,3-d{9 {8 1,4{9 OXAZEPIN-3-(2H)-ONES 失效
标题翻译： DIBENZA- {8 b，f {9 -S-三唑 - {8,3,3-d {9 {8 1,4 {9-氧杂-3-（2H） - 酮
公开(公告)号：US3853904A
公开(公告)日：1974-12-10
申请号：US38627873
申请日：1973-08-07
申请人： UPJOHN CO
发明人： SZMUSZKOVICZ J
IPC分类号： C07D267/20 , C07D487/04 , C07D498/04 , C07D99/02
CPC分类号： C07D487/04 , C07D267/20
摘要： Compounds of the formula III:

wherein R1 is selected from the group consisting of hydrogen, alkyl of 1 to 3 carbon atoms, inclusive and

IN WHICH R7 and R8 are hydrogen and alkyl, as defined above and n is 2 or 3, or together

IS PYRROLIDINO, PIPERIDINO OR N-methylpiperazino; wherein R3 and R4 are hydrogen, fluoro, chloro, bromo, nitro, alkyl defined as above, trifluoromethyl, or alkoxy, of 1 to 3 carbon atoms, inclusive, are prepared by reacting a thio compound of formula I:

wherein R3 and R4 are defined as above, in sequence; 1. WITH AN ALKYLCARBAZATE; AND THE RESULTING INTERMEDIATE PRODUCT II 2. with an alkylating agent of the formula R1''X in which R1'' is alkyl,

AS DEFINED ABOVE AND X is chlorine, bromine, or iodine, to obtain a compound III as defined above. Compounds of formula III and the pharmacologically acceptable acid addition salts thereof have anti-depressant activity and tranquilizing activity and can be used in mammals.
摘要翻译：式III化合物：

6. 发明授权

US3850942A 3-pyridyl-9h-dibenzo(c,f)-s-triazolo(4,3-a)azepine 失效
标题翻译： 3-吡啶基-9-二苯并（C，F）-S-三唑（4,3-A）
公开(公告)号：US3850942A
公开(公告)日：1974-11-26
申请号：US31320872
申请日：1972-12-08
申请人： UPJOHN CO
发明人： HESTER J , SZMUSZKOVICZ J
IPC分类号： A23K1/16 , C07D243/38 , C07D267/20 , C07D281/16 , C07D487/04 , C07D498/04 , C07D513/04 , C07D31/42
CPC分类号： C07D487/04 , C07D243/38 , C07D267/20 , C07D281/16 , C07D513/04
摘要： 1. 3-(2-PYRIDYL)-9H-DIBENZO(C,F)-S-TRIAZOLO(4,3-A) AZEPINE.

7. 发明授权

US3853882A 2,9-DIHYDRO-{8 c,f{9 -S-TRIAZOLO{8 4,3-a{9 AZEPIN-3-ONES 失效
标题翻译： 2,9-二氢 - {8c，f {9-S-TRIAZOLO {8,43-a {9 AZEPIN-3-ONES
公开(公告)号：US3853882A
公开(公告)日：1974-12-10
申请号：US38627773
申请日：1973-08-07
申请人： UPJOHN CO
发明人： SZMUSZKOVICZ J
IPC分类号： C07D487/04 , C07D57/02 , C07D99/02
CPC分类号： C07D487/04
摘要： Compounds of the formula III:

wherein R'' is hydrogen or methyl; wherein R1 is hydrogen, alkyl defined as above,

IN WHICH N IS 2 TO 3 AND R is alkyl of one to three carbon atoms, inclusive,

IN WHICH R7 and R8 are each selected from the group consisting of hydrogen and alkyl as defined above or

TOGETHER IS PYRROLIDINO AND PIPERIDINO; AND WHEREIN R3 and R4 are hydrogen, fluoro, chloro, bromo, nitro, alkyl defined as above, trifluoromethyl, or alkoxy, of one to three carbon atoms, inclusive, are prepared by reacting a thio compound of formula I:

wherein R'', R3, and R4 are defined as above, in sequence: 1. WITH AN ALKYLCARBAZATE; AND THE RESULTING PRODUCT II 2. with an alkylating agent of the formula R''1Cl or R1''Br in which R1'' is defined as R1 exclusive of hydrogen to obtain a compound III as defined above. Compounds of formula II and III and the pharmacologically acceptable acid addition salts thereof have antidepressant activity and can be used in mammals.
摘要翻译：式III化合物：

8. 发明授权

US3842080A 7-phenylpyrimido(1,2-a)(1,4)benzodiazepin-1(5h)-ones 失效
标题翻译：（1,2-A）（1,4）苯并咪唑-1-（5H） - 酮
公开(公告)号：US3842080A
公开(公告)日：1974-10-15
申请号：US32376673
申请日：1973-01-15
申请人： UPJOHN CO
发明人： SZMUSZKOVICZ J
IPC分类号： C07D487/04 , C07D53/06
CPC分类号： C07D487/04
摘要： 1. A 7-PHENYLPYRIMIDO(1,2-A)(1,4)BENZODIAZEPIN-1 (5H)-ONE OF THE FORMULA:

1-(O=),2-R10,5-R1,7-(R2,R3-PHENYL-),R4,R5-5H-PYRIMIDO-

(1,2-A)(1,4)BENZODIAZEPINE

WHEREIN RO IS SELECTED FROM THE GROUP CONSISTING OF HYDROGEN, METHYL, HYDROXYMETHYL, AND -COOR6 IN WHICH R6 IS HYDROGEN OR ALKYL OF 1 TO 3 CARBON ATOMS, INCLUSIVE; WHEREIN R1 IS SELECTED FROM THE GROUP CONSISTING OF HYDROGEN, HYDROXY, ACETOXY, PROPIONOXY, OR SUCCINYLOXY ALKYL ESTERS IN WHICH ALKYL IS DEFINED AS ABOVE; AND WHEREIN R2, R3, R5 ARE SELECTED FROM THE GROUP CONSISTING OF HYDROGEN, HALOGEN, NITRO, CYANO, TRIFLUOROMETHYL, AND ALKYL, ALKOXY, ALKYLTHIO, ALKYLSULFINYL, ALKYLSULFONYL, AND ALKANOYLAMINO IN WHICH THE CARBON MOIETY IS OF 1 TO 3 CARBON ATOMS, INCLUSIVE, AND DIALKYLAMINO IN WHICH ALKYL IS DEFINED AS ABOVE, THE PHARMACOLOGICALLY ACCEPTABLE ACID ADDITION SALTS THEREOF. THE N-OXIDES THEREOF.

你已经成功收藏专利！

检索式保存成功!

IPRDB

热门服务

关于我们

友情链接

联系方式