公开(公告)号：DE2022503A1

公开(公告)日：1971-11-25

申请号：DE2022503

申请日：1970-05-08

Applicant: HOECHST AG

Inventor： WOLF E ,  KOHL H ,  HERTFELDER G

IPC: C07F9/53 ,  C07F9/645 ,  C07F9/28

Abstract: The new cpds. are of formula (I) in which R1 and R2 are H, NO2, halogen, or CF3; R2 may be straight or branched 1-6C alkyl, r3 is 1-3C alkyl, and n is 1-6. The cpds. have potent tranquillising activity with the advantage that they form stable aq. soln. They may be prepared by reacting metal derivs. of benzodiazepines with X(CH2)nP(O)(R3)2 where X is halogen, alkylsulphonyl or arylsulphonyl.

公开(公告)号：SE325889B

公开(公告)日：1970-07-13

申请号：SE966566

申请日：1966-07-14

Applicant: HOECHST AG

Inventor： WOLF E ,  SCHRINNER E

IPC: A61K31/505 ,  C07D239/92 ,  C07D51/48

公开(公告)号：NZ223336A

公开(公告)日：1989-09-27

申请号：NZ22333688

申请日：1988-01-28

Applicant: HOECHST AG

Inventor： WOLF E ,  ROSSMANITH E ,  BARTLETT R R ,  SCHLEYERBACH R

IPC: A61K31/55 ,  A61P29/00 ,  A61P37/00 ,  C07D243/08

Abstract: 1-(4-Hydroxy-3,5-di-tert.-butylbenzoyl)homopiperazine and various derivatives thereof substituted on the nitrogen are prepared starting from 4-hydroxy-3,5-di-tert.-butylbenzoic acid or its derivatives and homopiperazine or appropriate derivatives thereof. The compounds and their physiologically tolerated acid addition salts are suitable for the treatment of inflammatory and painful, in particular inflammatory rheumatic, disorders.

公开(公告)号：IE35197B1

公开(公告)日：1975-12-10

申请号：IE57571

申请日：1971-05-07

Applicant: HOECHST AG

Inventor： WOLF E ,  KOHL H ,  HERTFELDER G

IPC: C07F9/53 ,  C07F9/645 ,  C07F9/28

Abstract: 1345443 Phosphorus-containing benzodiazepine derivatives FARBWERKE HOECHST AG 5 May 1971 [8 May 1970 23 Sept 1970] 13207/71 Heading C2P [Also in Division A5] The invention comprises a phosphorus-containing benzodiazepine derivative of the general formula wherein R 1 is H, NO 2 , a halogen atom, or CF 3 , R 2 is a straight or branched chain alkyl group having up to 8 carbon atoms, a hydrogen atom, a halogen atom, NO 2 or CF 3 , R 3 is a straight chain or branched chain alkyl group having up to 3 carbon atoms and n is an integer from 1 to 6: They may be obtained by (a) reacting a metal derivative of the formula wherein M is a metal cation with a phosphine oxide of the formula X(CH 2 ) n P(O)(R 3 ) 2 , wherein X is a halogen atom or an alkyl (or aryl-) sulphonyloxy group, or (b) by reacting a compound of the formula with a derivative of amino acetic acid (preferably an ester, e.g. an imino or ortho ester derivative) or (c) by reacting a compound of the above Formula IV with a halide or azide of a halogenoacetic acid, treating the product with ammonia and then cyclizing the compound so obtained. In reaction (a) the metal compound can first be formed by heating the appropriate 1-unsubstituted benzodiazepine with, e.g., Ca-, Na- or Li-hydride or with potassium tertbutylate or sodium methylate in an inert organic solvent and the product may then be formed directly by reaction with the compound X(CH 2 ) n P(O)(R 3 ) 2 in the same solvent without isolation of the metal derivative. The products are useful as tranquillizers.

公开(公告)号：IN137523B

公开(公告)日：1975-08-09

申请号：IN605CA1975

申请日：1975-03-25

Applicant: HOECHST AG

Inventor： HARTFELDER G ,  WOLF E ,  KOHL H

IPC: C07D53/06

公开(公告)号：GB1345443A

公开(公告)日：1974-01-30

申请号：GB1320771

申请日：1971-05-05

Applicant: HOECHST AG

Inventor： WOLF E ,  KOHL H ,  HERTFELDER G

IPC: C07F9/53 ,  C07F9/645 ,  C07F9/28 ,  A61K27/00

Abstract: 1345443 Phosphorus-containing benzodiazepine derivatives FARBWERKE HOECHST AG 5 May 1971 [8 May 1970 23 Sept 1970] 13207/71 Heading C2P [Also in Division A5] The invention comprises a phosphorus-containing benzodiazepine derivative of the general formula wherein R 1 is H, NO 2 , a halogen atom, or CF 3 , R 2 is a straight or branched chain alkyl group having up to 8 carbon atoms, a hydrogen atom, a halogen atom, NO 2 or CF 3 , R 3 is a straight chain or branched chain alkyl group having up to 3 carbon atoms and n is an integer from 1 to 6: They may be obtained by (a) reacting a metal derivative of the formula wherein M is a metal cation with a phosphine oxide of the formula X(CH 2 ) n P(O)(R 3 ) 2 , wherein X is a halogen atom or an alkyl (or aryl-) sulphonyloxy group, or (b) by reacting a compound of the formula with a derivative of amino acetic acid (preferably an ester, e.g. an imino or ortho ester derivative) or (c) by reacting a compound of the above Formula IV with a halide or azide of a halogenoacetic acid, treating the product with ammonia and then cyclizing the compound so obtained. In reaction (a) the metal compound can first be formed by heating the appropriate 1-unsubstituted benzodiazepine with, e.g., Ca-, Na- or Li-hydride or with potassium tertbutylate or sodium methylate in an inert organic solvent and the product may then be formed directly by reaction with the compound X(CH 2 ) n P(O)(R 3 ) 2 in the same solvent without isolation of the metal derivative. The products are useful as tranquillizers.

公开(公告)号：DD97348A5

公开(公告)日：1973-05-05

申请号：DD16473171

申请日：1971-05-07

Applicant: HOECHST AG

Inventor： WOLF E ,  KOHL H ,  HERTFELDER G

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

Abstract: 1345443 Phosphorus-containing benzodiazepine derivatives FARBWERKE HOECHST AG 5 May 1971 [8 May 1970 23 Sept 1970] 13207/71 Heading C2P [Also in Division A5] The invention comprises a phosphorus-containing benzodiazepine derivative of the general formula wherein R 1 is H, NO 2 , a halogen atom, or CF 3 , R 2 is a straight or branched chain alkyl group having up to 8 carbon atoms, a hydrogen atom, a halogen atom, NO 2 or CF 3 , R 3 is a straight chain or branched chain alkyl group having up to 3 carbon atoms and n is an integer from 1 to 6: They may be obtained by (a) reacting a metal derivative of the formula wherein M is a metal cation with a phosphine oxide of the formula X(CH 2 ) n P(O)(R 3 ) 2 , wherein X is a halogen atom or an alkyl (or aryl-) sulphonyloxy group, or (b) by reacting a compound of the formula with a derivative of amino acetic acid (preferably an ester, e.g. an imino or ortho ester derivative) or (c) by reacting a compound of the above Formula IV with a halide or azide of a halogenoacetic acid, treating the product with ammonia and then cyclizing the compound so obtained. In reaction (a) the metal compound can first be formed by heating the appropriate 1-unsubstituted benzodiazepine with, e.g., Ca-, Na- or Li-hydride or with potassium tertbutylate or sodium methylate in an inert organic solvent and the product may then be formed directly by reaction with the compound X(CH 2 ) n P(O)(R 3 ) 2 in the same solvent without isolation of the metal derivative. The products are useful as tranquillizers.

公开(公告)号：SE352343B

公开(公告)日：1972-12-27

申请号：SE1552770

申请日：1970-07-31

Applicant: HOECHST AG

Inventor： KOENIG W ,  GEIGER R ,  WOLF E

IPC: A61K38/00 ,  C07D253/08 ,  C07K1/10 ,  C07K5/068 ,  C07K14/695 ,  C07C103/52

Abstract: 1318963 1,2,3 - Benzo triazines FARBWERKE HOECHST AG 3 Aug 1970 [1 Aug 1969] 37320/70 Heading C2C A 3 - hydroxy - 4 - oxo - 3,4 - dihydro - 1,2,3- benzo triazine ester of a protected amino acid or a protected peptide, which is prepared from the free 3-hydroxy benzo triazine and a protected amino acid or peptide containing a free carboxyl group in the presence of a carbo diimide, is used in the preparation of peptides wherein a carboxylic ester of a protected amino acid or peptide is reacted with an amino acid or peptide having a free amino group and protecting groups are subsequently removed. The following starting materials are prepared. Z - Asn(Mbh)OH, Z - Gln(Mbh)OH and its methyl ester and H Gln(Mbh)OMe, HCl, Z-Gly- NH-MbH, and BOC-Leu-Phe-OH, where "Mbh" is 4,4 1 -dimethoxy benzhydryl.

公开(公告)号：DE2046848A1

公开(公告)日：1972-03-30

申请号：DE2046848

申请日：1970-09-23

Applicant: HOECHST AG

Inventor： WOLF E ,  KOHL H ,  HERTFELDER G

IPC: C07F9/53 ,  C07F9/645 ,  C07F9/28

Abstract: The new cpds. are of formula (I) in which R1 and R2 are H, NO2, halogen, or CF3; R2 may be straight or branched 1-6C alkyl, r3 is 1-3C alkyl, and n is 1-6. The cpds. have potent tranquillising activity with the advantage that they form stable aq. soln. They may be prepared by reacting metal derivs. of benzodiazepines with X(CH2)nP(O)(R3)2 where X is halogen, alkylsulphonyl or arylsulphonyl.

公开(公告)号：NL7106239A

公开(公告)日：1971-11-10

申请号：NL7106239

申请日：1971-05-06

Applicant: HOECHST AG

Inventor： WOLF E ,  KOHL H ,  HERTFELDER G

IPC: C07F9/53 ,  C07F9/645 ,  C07F9/28 ,  A61K27/00

Abstract: 1345443 Phosphorus-containing benzodiazepine derivatives FARBWERKE HOECHST AG 5 May 1971 [8 May 1970 23 Sept 1970] 13207/71 Heading C2P [Also in Division A5] The invention comprises a phosphorus-containing benzodiazepine derivative of the general formula wherein R 1 is H, NO 2 , a halogen atom, or CF 3 , R 2 is a straight or branched chain alkyl group having up to 8 carbon atoms, a hydrogen atom, a halogen atom, NO 2 or CF 3 , R 3 is a straight chain or branched chain alkyl group having up to 3 carbon atoms and n is an integer from 1 to 6: They may be obtained by (a) reacting a metal derivative of the formula wherein M is a metal cation with a phosphine oxide of the formula X(CH 2 ) n P(O)(R 3 ) 2 , wherein X is a halogen atom or an alkyl (or aryl-) sulphonyloxy group, or (b) by reacting a compound of the formula with a derivative of amino acetic acid (preferably an ester, e.g. an imino or ortho ester derivative) or (c) by reacting a compound of the above Formula IV with a halide or azide of a halogenoacetic acid, treating the product with ammonia and then cyclizing the compound so obtained. In reaction (a) the metal compound can first be formed by heating the appropriate 1-unsubstituted benzodiazepine with, e.g., Ca-, Na- or Li-hydride or with potassium tertbutylate or sodium methylate in an inert organic solvent and the product may then be formed directly by reaction with the compound X(CH 2 ) n P(O)(R 3 ) 2 in the same solvent without isolation of the metal derivative. The products are useful as tranquillizers.