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1. 发明专利

TW012597B 特定之結合蛋白質及其對應之可結合性基質之測定方法失效
简体标题：特定之结合蛋白质及其对应之可结合性基质之测定方法
公开(公告)号：TW012597B
公开(公告)日：1973-05-01
申请号：TW019648
申请日：1971-12-15
申请人： N.V. ORGANON
发明人： DR. ANTOMOUS HERMANUS WILHELMU
IPC分类号： A61K

2. 实用新型

TW001917U 碳欠固醇(C NOR STEROID) 失效
公开(公告)号：TW001917U
公开(公告)日：1963-02-01
申请号：TW004536
申请日：1961-12-27
申请人： N.V. ORGANON
发明人： GUY HENRI OURISSON , MAX SALOMON DE WINTER , REINIER HENDRILCUS VAN DEN BOS
IPC分类号： C07J

3. 发明专利

DE1944048B2 未知
公开(公告)号：DE1944048B2
公开(公告)日：1973-10-31
申请号：DE1944048
申请日：1969-08-29
申请人： N.V. ORGANON, OSS (NIEDERLANDE)
发明人： MOELKER, HUIBERT CORNELIS THEUES, OSS (NIEDERLANDE)
IPC分类号： C12N11/06 , C11D3/386 , C12N11/02 , C12N11/18 , C12P21/02 , C07G7/02

4. 发明专利

DE2147799B2 未知
公开(公告)号：DE2147799B2
公开(公告)日：1981-02-26
申请号：DE2147799
申请日：1971-09-24
申请人： N.V. ORGANON, OSS (NIEDERLANDE)
发明人： WIED, DAVID DE, PROF. DR., BILTHOVEN (NIEDERLANDE)
IPC分类号： C07K7/16 , A61K37/02
摘要： 1342803 Peptides ORGANON LABORATORIES Ltd 14 Sept 1971 [26 Sept 1970] 42869/71 Heading C2C [Also in Division A5] The following reaction sequences are disclosed (Al) Z-Pro-OH. (Z is benzyloxycarbonyl) and H - Lys(tosyl) - OCH 3 .HCl give Z - Pro- Lys(tosyl) - OCH 3 . (A2) This product is hydrogenated in HCl to H-Pro-Lys(tosyl)- OCH 3 .HCl. (A3) This product is reacted with Z - Glu(NH 2 ) - Asp(NH 2 ) - Cys(benzyl) - OH to give Z - Gln - Asn - Cys(benzyl - Pro - Lys- (tosyl)-OCH 3 (A4) This product is saponified to give Z - Gln - Asn - Cys(benzyl) - Pro - Lys (tosyl)-OH. (A5. 1) This product is hydrogenated to H-Gln-Asn-Cys(benzyl)-Pro-Lys(tosyl)- OH. (A5. 2) Z - Gln . Asn - Cys(benzyl) - Pro- Lys(tosyl)-OCH 3 is hydrogenated to H-Gln- Asn - Cys(benzyl) - Pro - Lys(tosyl) - OCH3. Example I Z.Cys(benzyl)-Tyr-Phe-N 2 H 3 is reacted with H - Gln - Asn . Cys(benzyl) - Pro- Lys(tosyl)-OH.HCl and all protecting groups removed to give Similar reactions are also disclosed in which lysine is replaced by arginine. (B1-B5 and Example II). Hydrochloride, phosphate and maleates of the final products are prepared.

5. 发明专利

DE2016783C3 未知
公开(公告)号：DE2016783C3
公开(公告)日：1978-06-08
申请号：DE2016783
申请日：1970-04-08
申请人： N.V. ORGANON, OSS (NIEDERLANDE)
发明人： GORP, JACOBUS ANTONIUS VAN , REE, PIETER JURIANUS VAN
IPC分类号： C07J1/00
摘要： 1304415 Preparation of 17α-hydroxy or acyloxyandrostane compounds ORGANON LABORATORIES Ltd 1 April 1970 [8 April 1969] 15371/70 Heading C2U A 17α-acyloxy or 17α-hydroxy steroid is prepared by reacting a 17#-sulphonyloxy steroid, derived from any organic sulphonic acid, with an alkali metal salt of a C 1-6 aliphatic carboxylic acid in the presence of a C 1-6 aliphatic carboxylic acid and an aprotic solvent and, when required, hydrolysing the 17α-acyloxy steroid first formed to the free 17α-hydroxy steroid. Suitable starting materials are sulphonates of testosterone, 19-nortestosterone, estradiol, 17#-dihydroequilin and 17#-dihydroequilenin. The sulphonyloxy steroids can for example be derived from alkyl-, aryl- or aralkyl-sulphonic acids. If the alkali metal salt reagent is derived from an acid different from the free acid reagent used then a mixture of different 17α-acyloxy products is formed. The preferred solvent is dimethylformamide.

6. 发明专利

DE1944048C3 未知
公开(公告)号：DE1944048C3
公开(公告)日：1974-06-27
申请号：DE1944048
申请日：1969-08-29
申请人： N.V. ORGANON, OSS (NIEDERLANDE)
发明人： MOELKER, HUIBERT CORNELIS THEUES, OSS (NIEDERLANDE)
IPC分类号： C12N11/06 , C11D3/386 , C12N11/02 , C12N11/18 , C12P21/02 , C07G7/02 , A61K7/00 , A61K19/00 , C11D7/42

7. 发明专利

DE1543273C3 未知
公开(公告)号：DE1543273C3
公开(公告)日：1974-02-21
申请号：DE1543273
申请日：1965-06-15
申请人： N.V. ORGANON, OSS (NIEDERLANDE)
发明人： JONGH, HENDRIK PAUL DE , VLIET, NICOLAAS PIETER VAN
IPC分类号： A61K31/565 , A61K31/566 , A61K31/567 , C07J1/00 , C07J75/00 , C07C169/10

8. 发明专利

DE1695556B2 未知
公开(公告)号：DE1695556B2
公开(公告)日：1980-10-30
申请号：DE1695556
申请日：1967-03-09
申请人： N.V. ORGANON, OSS (NIEDERLANDE)
发明人： BURG, WILLEM JACOB VAN DER, OSS , DELOBELLE, JACQUES, DR., GISORS
IPC分类号： C07D241/04 , C07D471/04 , C07D487/04 , A61K31/55
摘要： 1,173,783. Fused-ring piperazine derivatives. ORGANON LABORATORIES Ltd. 9 March, 1967 [12 March, 1966], No. 11168/67. Heading C2C. Novel fused-ring piperazine derivatives of the general formula wherein R 1 and R 3 are each a hydrogen or halogen atom, a hydroxy, C 1-6 acyloxy, C 1-6 alkyl, C 1-6 alkoxy or trifluoromethyl group; R 2 is a hydrogen atom or a C 1-6 alkyl or aralkyl group, or an aminoethyl or aminopropyl N- substituted by one or more C 1-6 alkyl groups, or a C 1-6 alkyl group attached to a N-containing heterocyclic ring, said ring being directly bonded to the N atom of the piperazine ring; and P is a single bond or a methylene, ethylene or -CH= CH- group; and acid addition salts thereof are prepared by reduction of the corresponding piperazinones having keto groups in at least one of the positions 3, 5 and 6 of the piperazine ring, followed by optional conversion to an acid addition salt of the product. The piperazinone starting materials are prepared (a) by reaction of an amine of the formula with a compound of the formula wherein X is a halogen or a C 1-6 alkoxy group and Z is two hydrogen atoms or an oxygen atom, to give a 5-keto-, 6-keto- or 5,6-diketopiperazine derivative; or (b) by reaction of an amine of the second formula above, wherein R 2 is hydrogen with benzyl chloroformate, followed by reaction of the product with a halogenated acetic acid halide, removal of the benzyloxycarbonyl group by catalytic reduction and closure of the piperazine ring at an elevated temperature. 6 - Chloromethyl - morphanthridine and 2 - bromo - 6 - chloromethyl - phenanthridine are prepared by ring closure methods from N- chloroacetyl - 2 - benzylaniline and N - chloroacetyl - 2 - phenyl - 4 - bromoaniline, respectively. 6 - Cyanodibenzo - (b,f) - azocine is prepared by reaction of 6-chlorodibenzo-(b,f)- azocine with sodium cyanide. 6-Formylaminomethyl - 5,6 - dihydro - dibenzo - (b,f) - azocine is prepared by the action of methyl formate on 6 - aminomethyl - 5,6 - dihydrodibenzo - (b,f)- azocine. Pharmaceutical compositions having antiinflammatory, -serotoninic, -histaminic and -phlogistic activity comprise a fused-ring piperazine derivative of the first formula above or an acid addition salt thereof as active ingredient, together with at least one pharmaceutical carrier.

9. 发明专利

DE1518058C3 未知
公开(公告)号：DE1518058C3
公开(公告)日：1974-02-21
申请号：DE1518058
申请日：1964-03-06
申请人： N.V. ORGANON, OSS (NIEDERLANDE)
发明人： BEYERMAN, HUGO CHRISTIAAN, DR., WASSENAAR , BRINK, WILLEM MAASSEN, VAN DEN, SCHIEDAM
IPC分类号： B01J31/02 , C07K1/08 , C07K5/06 , C07K5/083 , C07K5/103 , C07C103/52

10. 发明专利

DE1795836C2 未知
公开(公告)号：DE1795836C2
公开(公告)日：1978-07-20
申请号：DE1795836
申请日：1967-03-09
申请人： N.V. ORGANON, OSS (NIEDERLANDE)
发明人： BURG, WILLEM JACOB VAN DER, OSS , DELOBELLE, JACQUES, DR., GISORS
IPC分类号： C07D241/04 , C07D471/04 , C07D487/04 , A61K31/00
摘要： 1,173,783. Fused-ring piperazine derivatives. ORGANON LABORATORIES Ltd. 9 March, 1967 [12 March, 1966], No. 11168/67. Heading C2C. Novel fused-ring piperazine derivatives of the general formula wherein R 1 and R 3 are each a hydrogen or halogen atom, a hydroxy, C 1-6 acyloxy, C 1-6 alkyl, C 1-6 alkoxy or trifluoromethyl group; R 2 is a hydrogen atom or a C 1-6 alkyl or aralkyl group, or an aminoethyl or aminopropyl N- substituted by one or more C 1-6 alkyl groups, or a C 1-6 alkyl group attached to a N-containing heterocyclic ring, said ring being directly bonded to the N atom of the piperazine ring; and P is a single bond or a methylene, ethylene or -CH= CH- group; and acid addition salts thereof are prepared by reduction of the corresponding piperazinones having keto groups in at least one of the positions 3, 5 and 6 of the piperazine ring, followed by optional conversion to an acid addition salt of the product. The piperazinone starting materials are prepared (a) by reaction of an amine of the formula with a compound of the formula wherein X is a halogen or a C 1-6 alkoxy group and Z is two hydrogen atoms or an oxygen atom, to give a 5-keto-, 6-keto- or 5,6-diketopiperazine derivative; or (b) by reaction of an amine of the second formula above, wherein R 2 is hydrogen with benzyl chloroformate, followed by reaction of the product with a halogenated acetic acid halide, removal of the benzyloxycarbonyl group by catalytic reduction and closure of the piperazine ring at an elevated temperature. 6 - Chloromethyl - morphanthridine and 2 - bromo - 6 - chloromethyl - phenanthridine are prepared by ring closure methods from N- chloroacetyl - 2 - benzylaniline and N - chloroacetyl - 2 - phenyl - 4 - bromoaniline, respectively. 6 - Cyanodibenzo - (b,f) - azocine is prepared by reaction of 6-chlorodibenzo-(b,f)- azocine with sodium cyanide. 6-Formylaminomethyl - 5,6 - dihydro - dibenzo - (b,f) - azocine is prepared by the action of methyl formate on 6 - aminomethyl - 5,6 - dihydrodibenzo - (b,f)- azocine. Pharmaceutical compositions having antiinflammatory, -serotoninic, -histaminic and -phlogistic activity comprise a fused-ring piperazine derivative of the first formula above or an acid addition salt thereof as active ingredient, together with at least one pharmaceutical carrier.

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