公开(公告)号：US3725404A

公开(公告)日：1973-04-03

申请号：US3725404D

申请日：1971-06-09

Applicant: HOECHST AG

Inventor： KUCH H ,  SCHMITT K ,  SEIDL G ,  HOFFMANN I

IPC: C07D265/18 ,  C07D87/20

CPC classification number: C07D265/18

Abstract: 2-Amino-4,4-di-substituted benzoxazine derivatives and the salts thereof with a physiologically compatible acid have an action on the central nervous system. These benzoxazines have the formula IN WHICH R is hydrogen, alkyl of one to four carbon atoms, cyclohexyl, phenyl or benzyl, R1 is hydrogen, halogen, trifluoromethyl, R2 is alkyl of one to four carbon atoms and R3 is phenyl or halophenyl.

Abstract translation: 2-氨基-4,4-二取代苯并恶嗪衍生物及其与生理上相容的酸的盐对中枢神经系统具有作用。 这些苯并恶嗪具有下式：其中R是氢，1-4个碳原子的烷基，环己基，苯基或苄基，R1是氢，卤素，三氟甲基，R2是1-4个碳原子的烷基，R3是苯基或卤代苯基。

公开(公告)号：US3718645A

公开(公告)日：1973-02-27

申请号：US3718645D

申请日：1971-05-06

Applicant: HOECHST AG

Inventor： KUCH H ,  HOFFMANN I

IPC: C07D243/12 ,  C07F9/53 ,  C07F9/645 ,  C07D53/04

CPC classification number: C07F9/645 ,  C07F9/5304

Abstract: Dialkylphosphinylalkylene-substituted 1,5-benzodiazepines useful as medicaments in the treatment of psychic diseases are obtainable by reacting the corresponding benzodiazepines with a dialkyl-phosphinylalkyl halide or by reacting a 2-dialkylphosphinylalkylaminodiphenylamine with a malonic acid dihalide or alkylmalonic acid dihalide.

Abstract translation: 可用作治疗心理疾病的药物的二烷基亚膦基亚烷基亚烷基取代的1,5-苯并二氮杂通过使相应的苯并二氮杂与二烷基 - 膦基烷基卤化物反应或通过使2-二烷基 - 亚膦基烷基氨基二苯胺与丙二酸二卤化物或烷基丙二酸二卤化物反应来获得。

公开(公告)号：BG20373A3

公开(公告)日：1975-11-05

申请号：BG2363272

申请日：1972-04-11

Applicant: HOECHST AG

Inventor： KUCH H ,  HOFFMANN I

IPC: C07D243/12 ,  C07F9/53 ,  C07F9/645 ,  C07D53/04

Abstract: Dialkylphosphinylalkylene-substituted 1,5-benzodiazepines useful as medicaments in the treatment of psychic diseases are obtainable by reacting the corresponding benzodiazepines with a dialkyl-phosphinylalkyl halide or by reacting a 2-dialkyl-phosphinylalkylaminodiphenylamine with a malonic acid dihalide or alkylmalonic acid dihalide.

公开(公告)号：SE357563B

公开(公告)日：1973-07-02

申请号：SE1614767

申请日：1967-11-24

Applicant: HOECHST AG

Inventor： KUCH H ,  SCHMITT K ,  SEIDL G ,  HOFFMANN I

IPC: A61K31/00 ,  C07D93/08

Abstract: 1,214,000. Benzothiazine derivatives. FARBWERKE HOECHST A.G. 27 Nov., 1967 [26 Nov., 1966], No. 53960/67. Heading C2C. Compounds of the general formula (R = H, alkyl, cycloalkyl, alkenyl, cycloalkenyl, aryl, aralkyl, lower dialkylaminoalkyl, or lower aminoalkyl in which the amino group has the formula A#N-, A representing an alkylene group that may be interrupted by O, S, methylimino or benzylimino; R 1 = H, halogen, OMe, CF 3 or NO 2 ; R 2,3 = alkyl, cycloalkyl, phenylalkyl or phenyl, in which the phenyl group or the phenyl residue of the phenylalkyl group may be substituted by one or more substituents selected from halogen, OMe, CF 3 and NO 2 ) and their acid addition salts are prepared by (a) reacting a compound of the formula (X = Cl, Br, OH, SH, alkoxy, alkylthio or alkanoyloxy) or a salt thereof with (R values identical or different) or R.NCS or a compound capable of forming such an isothiocyanate, if necessary or desired in the presence of an acid and/or a dehydrating agent, (b) reacting a compound of the formula or a functional derivative thereof with an inorganic sulphide or, if X = SH or alkylthio, with a dehydrating agent, if necessary or desired in the presence of an acid, (c) reacting a compound of the formula (R 4 = Cl, Br, amino, SH or alkylthio) with R 1 NH 2 (R 1 = R other than H) or a salt thereof, or (d) reducing with a complex metal hydride or saponifying a compound of the formula (R 11 = alkyl, alkenyl, aryl, aralkyl, haloalkyl, lower dialkylaminoalkyl, or lower aminoalkyl in which the amino group has the formula A#N-), the compound being reacted, before or after reduction of the acyl group, with a dialkylamine or an appropriate cyclic amine in cases where R 11 = haloalkyl, optionally followed in each case by salt formation. The, lower dialkylaminoalkyl and aminoalkyl groups (excluding any interrupting methylimino or benzylimino group in the latter case) contain up to ten carbon atoms. The isolation of intermediate thiourea derivatives in process (a) is described. The above compounds possess a depressive effect on the central nervous system, a stimulating, tranquillizing and narcosis-prolonging activity and analgesic and spasmolytic activity. They may be administered in the form of pharmaceutical preparations containing them in association with a carrier.

公开(公告)号：BE782213A

公开(公告)日：1972-10-17

申请号：BE782213

申请日：1972-04-17

Applicant: HOECHST AG

Inventor： KUCH H ,  HOFFMANN I

IPC: C07D243/12 ,  C07F9/53 ,  C07F9/645 ,  C07F ,  A61K

Abstract: Dialkylphosphinylalkylene-substituted 1,5-benzodiazepines useful as medicaments in the treatment of psychic diseases are obtainable by reacting the corresponding benzodiazepines with a dialkyl-phosphinylalkyl halide or by reacting a 2-dialkyl-phosphinylalkylaminodiphenylamine with a malonic acid dihalide or alkylmalonic acid dihalide.

公开(公告)号：EG10547A

公开(公告)日：1976-06-30

申请号：EG14372

申请日：1972-04-11

Applicant: HOECHST AG

Inventor： KUCH H ,  HOFFMANN I

IPC: C07D243/12 ,  C07F9/53 ,  C07F9/645 ,  A61K31/675

Abstract: Dialkylphosphinylalkylene-substituted 1,5-benzodiazepines useful as medicaments in the treatment of psychic diseases are obtainable by reacting the corresponding benzodiazepines with a dialkyl-phosphinylalkyl halide or by reacting a 2-dialkyl-phosphinylalkylaminodiphenylamine with a malonic acid dihalide or alkylmalonic acid dihalide.

公开(公告)号：BG20110A3

公开(公告)日：1975-10-30

申请号：BG2019572

申请日：1972-04-11

Applicant: HOECHST AG

Inventor： KUCH H ,  HOFFMANN I

IPC: C07D243/12 ,  C07F9/53 ,  C07F9/645 ,  C07D53/04

Abstract: Dialkylphosphinylalkylene-substituted 1,5-benzodiazepines useful as medicaments in the treatment of psychic diseases are obtainable by reacting the corresponding benzodiazepines with a dialkyl-phosphinylalkyl halide or by reacting a 2-dialkyl-phosphinylalkylaminodiphenylamine with a malonic acid dihalide or alkylmalonic acid dihalide.

公开(公告)号：SE373857B

公开(公告)日：1975-02-17

申请号：SE587571

申请日：1971-05-06

Applicant: HOECHST AG

Inventor： KUCH H ,  HOFFMANN I

IPC: C07F9/53 ,  C07F9/645 ,  C07D243/12 ,  C07D53/04 ,  C07F9/50

Abstract: Dialkylphosphinylalkylene-substituted 1,5-benzodiazepines useful as medicaments in the treatment of psychic diseases are obtainable by reacting the corresponding benzodiazepines with a dialkyl-phosphinylalkyl halide or by reacting a 2-dialkyl-phosphinylalkylaminodiphenylamine with a malonic acid dihalide or alkylmalonic acid dihalide.

公开(公告)号：NO130685C

公开(公告)日：1975-01-22

申请号：NO17066667

申请日：1967-11-23

Applicant: HOECHST AG

Inventor： KUCH H ,  SCHMITT K ,  SEIDL G ,  HOFFMANN I

IPC: A61K31/00 ,  C07D93/08

Abstract: 1,214,000. Benzothiazine derivatives. FARBWERKE HOECHST A.G. 27 Nov., 1967 [26 Nov., 1966], No. 53960/67. Heading C2C. Compounds of the general formula (R = H, alkyl, cycloalkyl, alkenyl, cycloalkenyl, aryl, aralkyl, lower dialkylaminoalkyl, or lower aminoalkyl in which the amino group has the formula A#N-, A representing an alkylene group that may be interrupted by O, S, methylimino or benzylimino; R 1 = H, halogen, OMe, CF 3 or NO 2 ; R 2,3 = alkyl, cycloalkyl, phenylalkyl or phenyl, in which the phenyl group or the phenyl residue of the phenylalkyl group may be substituted by one or more substituents selected from halogen, OMe, CF 3 and NO 2 ) and their acid addition salts are prepared by (a) reacting a compound of the formula (X = Cl, Br, OH, SH, alkoxy, alkylthio or alkanoyloxy) or a salt thereof with (R values identical or different) or R.NCS or a compound capable of forming such an isothiocyanate, if necessary or desired in the presence of an acid and/or a dehydrating agent, (b) reacting a compound of the formula or a functional derivative thereof with an inorganic sulphide or, if X = SH or alkylthio, with a dehydrating agent, if necessary or desired in the presence of an acid, (c) reacting a compound of the formula (R 4 = Cl, Br, amino, SH or alkylthio) with R 1 NH 2 (R 1 = R other than H) or a salt thereof, or (d) reducing with a complex metal hydride or saponifying a compound of the formula (R 11 = alkyl, alkenyl, aryl, aralkyl, haloalkyl, lower dialkylaminoalkyl, or lower aminoalkyl in which the amino group has the formula A#N-), the compound being reacted, before or after reduction of the acyl group, with a dialkylamine or an appropriate cyclic amine in cases where R 11 = haloalkyl, optionally followed in each case by salt formation. The, lower dialkylaminoalkyl and aminoalkyl groups (excluding any interrupting methylimino or benzylimino group in the latter case) contain up to ten carbon atoms. The isolation of intermediate thiourea derivatives in process (a) is described. The above compounds possess a depressive effect on the central nervous system, a stimulating, tranquillizing and narcosis-prolonging activity and analgesic and spasmolytic activity. They may be administered in the form of pharmaceutical preparations containing them in association with a carrier.

公开(公告)号：BR7202216D0

公开(公告)日：1973-07-17

申请号：BR221672

申请日：1972-04-14

Applicant: HOECHST AG

Inventor： KUCH H ,  HOFFMANN I

IPC: C07D243/12 ,  C07F9/53 ,  C07F9/645 ,  C07D53/04 ,  C07F9/28 ,  A61K27/00

Abstract: Dialkylphosphinylalkylene-substituted 1,5-benzodiazepines useful as medicaments in the treatment of psychic diseases are obtainable by reacting the corresponding benzodiazepines with a dialkyl-phosphinylalkyl halide or by reacting a 2-dialkyl-phosphinylalkylaminodiphenylamine with a malonic acid dihalide or alkylmalonic acid dihalide.