公开(公告)号：CH572066A5

公开(公告)日：1976-01-30

申请号：CH1345375

申请日：1972-04-12

Applicant: HOECHST AG

Inventor： KUCH H ,  HOFFMANN I

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

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：CH570414A5

公开(公告)日：1975-12-15

申请号：CH535772

申请日：1972-04-12

Applicant: HOECHST AG

Inventor： KUCH H ,  HOFFMANN I

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

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：FI48595B

公开(公告)日：1974-07-31

申请号：FI316967

申请日：1967-11-24

Applicant: HOECHST AG

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

IPC: C07D265/18 ,  C07D87/20

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.

公开(公告)号：ZA722518B

公开(公告)日：1973-01-31

申请号：ZA722518

申请日：1972-04-14

Applicant: HOECHST AG

Inventor： KUCH H ,  HOFFMANN I

IPC: C07F9/53 ,  C07D243/12 ,  C07F9/645 ,  C07D

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：FR2133751A1

公开(公告)日：1972-12-01

申请号：FR7213212

申请日：1972-04-14

Applicant: HOECHST AG

Inventor： KUCH H ,  HOFFMANN I

IPC: C07F9/53 ,  C07F9/645 ,  C07D243/12 ,  A61K27/00 ,  C07F9/00

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.

公开(公告)号：ZA804959B

公开(公告)日：1981-08-26

申请号：ZA804959

申请日：1980-08-13

Applicant: HOECHST AG

Inventor： RACKUR G ,  HOFFMANN I

IPC: A61K31/55 ,  A61P25/20 ,  C07D231/00 ,  C07D231/38 ,  C07D231/40 ,  C07D243/00 ,  C07D487/04 ,  C07D

Abstract: Compound of the general formula I in which R1 and R2 are identical or different and represent hydrogen atoms or alkyl groups with 1-6 C atoms, it also being possible for one of the radicals R1 and R2 to be, in each case, a benzyl, trifluoromethyl or phenyl group, R3 denotes a hydrogen atom, an alkyl group which has 1-6 C atoms and is optionally substituted by an aryl group, an alkoxy group with 1-6 C atoms, a trifluoromethyl group, a dialkylamino group with 2-12 C atoms or a cycloalkyl group with 3-6 C atoms, an alkenyl or alkynyl group with 2-6 C atoms, a cycloalkyl group with 3-6 C atoms or a carbalkoxy group with 2-6 C atoms, R4 is a hydrogen atom and R5 can be a phenyl group, a phenyl group which is monosubstituted or disubstituted by methyl Cl, Br, F, nitro, cyano and or trifluoromethyl or a pyridyl group and medicaments containing same.

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.