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1. 发明专利

PL80327B1 未知
公开(公告)号：PL80327B1
公开(公告)日：1975-08-30
申请号：PL13666269
申请日：1969-11-03
IPC分类号： C07D211/64 , C07D211/34 , C07D29/32
摘要： 1,234,359. Isonipecotic acid derivative. JANSSEN PHARMACEUTICA N.V. 31 Oct., 1969 [4 Nov., 1968], No. 53573/69. Heading C2C. The novel compound, 1 - (3 - cyano - 3,3- diphenylpropyl) - 4 - phenylisonipecotic acid, and its pharmaceutically acceptable acid addition salts, are prepared by hydrolysing a C 1-7 alkyl ester of said acid, and, if desired, converting the resulting acid into a pharmaceutically acceptable acid addition salt thereof. Pharmaceutical compositions having antidiarrheal and analgesic activity comprise the novel compound, or a pharmaceutically acceptable acid addition salt thereof, together with a pharmaceutical carrier. The compositions may be administered orally or parenterally, e.g. in the form of tablets, capsules, powders, suspensions, elixirs and solutions. Reference has been directed by the Comptroller to Specification 843,319.

2. 发明授权

US3790581A N-(1-(3-cyano-3,3-bis(optionally substituted phenyl)propyl)-4-phenylpiperidine-4-carbonyloxy)succinimides 失效
标题翻译： N-（1-（3-氰基-3,3-双（取代的苯基）丙基）-4-苯基哌啶-4-羰基）
公开(公告)号：US3790581A
公开(公告)日：1974-02-05
申请号：US3790581D
申请日：1972-08-17
申请人： SEARLE & CO
发明人： KREIDER E
IPC分类号： C07D211/64 , C07D29/32
CPC分类号： C07D211/64
摘要： PREPARATION OF THE SUBJECT COMPOUNDS BY REACTION OF 1-(3-CYANO-3,3-BIS(OPTIONALLY SUBSTITUTED PHENYL) PROPYL)4-PHENYLPIPERIDINE-4-CATBOXYLIC ACID WITH AN N-HYDROXY

HO-N
WHEREIN

-N
REPRESENTS AN OPTIONALLY SUBSTITUTED MONOCYCLIC OR FUSED POLYCYCLIC-HETEROCYCLIC RADICAL CONTAINING AT LEAST ONE CARBONYL FUNCTION ADJACENT TO THE NITROGEN ATOM, IN THE PRESENCE OF A SUITABLE DEHYDRATING AGENT, AND THEIR UNEXPECTED UTILITY AS NARCOTIC ANTAGONISTS ARE DISCLOSED.

3. 发明授权

US3853891A N-(n-(cyanoalkyl)-n-nitroso)amino-aminoalcohol 失效
标题翻译： N-（N-（氰基烷基）-N-硝基）氨基 - 氨基醇
公开(公告)号：US3853891A
公开(公告)日：1974-12-10
申请号：US37193273
申请日：1973-06-20
申请人： SANDOZ AG
发明人： SIMPSON W
IPC分类号： C07D295/28 , C07D29/32
CPC分类号： C07D295/30
摘要： Organic acid, halogenated organic acid and nitrate esters of N(N-(cyanoalkyl)-N-nitroso)amino-aminoalcohols, e.g., 4-(N-(1cyanoethyl)-N-nitroso)amino-1-piperazine-ethanol nitrate, are useful as anti-anginal agents.
摘要翻译： N-（N- [氰基烷基] -N-亚硝基）氨基 - 氨基醇的有机酸，卤代有机酸和硝酸酯，例如4-（N- [1-氰乙基] -N-亚硝基）氨基-1-哌嗪 - 乙醇硝酸盐可用作抗心绞痛剂。

4. 发明授权

US3534048A 2,2-dimethyl-4,4,6,6-tetrasubstituted-piperidine-1-oxide derivatives 失效
标题翻译： 2,2-二甲基-4,4,6,6-四取代哌啶-1-氧化物衍生物
公开(公告)号：US3534048A
公开(公告)日：1970-10-13
申请号：US3534048D
申请日：1967-06-01
申请人： SANKYO CO
发明人： MURAYAMA KEISUKE , MORIMURA SYOJI , YOSHIOKA TAKAO , HIGASIDA SUSUMU , YAMAO EIKO
IPC分类号： C07D211/94 , C07D221/20 , C07D471/10 , C07D29/30 , C07D29/32
CPC分类号： C07D221/20 , C07D211/94 , C07D471/10

6. 发明专利

IE33602B1 ISONIPECOTIC ACID DERIVATIVES AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM 未知
公开(公告)号：IE33602B1
公开(公告)日：1974-08-21
申请号：IE142769
申请日：1969-10-17
申请人： JANSSEN PHARMACEUTICA NV
IPC分类号： C07D211/64 , C07D211/34 , C07D29/32
摘要： 1,234,359. Isonipecotic acid derivative. JANSSEN PHARMACEUTICA N.V. 31 Oct., 1969 [4 Nov., 1968], No. 53573/69. Heading C2C. The novel compound, 1 - (3 - cyano - 3,3- diphenylpropyl) - 4 - phenylisonipecotic acid, and its pharmaceutically acceptable acid addition salts, are prepared by hydrolysing a C 1-7 alkyl ester of said acid, and, if desired, converting the resulting acid into a pharmaceutically acceptable acid addition salt thereof. Pharmaceutical compositions having antidiarrheal and analgesic activity comprise the novel compound, or a pharmaceutically acceptable acid addition salt thereof, together with a pharmaceutical carrier. The compositions may be administered orally or parenterally, e.g. in the form of tablets, capsules, powders, suspensions, elixirs and solutions. Reference has been directed by the Comptroller to Specification 843,319.

7. 发明专利

GB1348165A N-N-CYANOALKYL-N-NITROSO-AMINO-AMINO-ALCOHOL ESTERS 未知
公开(公告)号：GB1348165A
公开(公告)日：1974-03-13
申请号：GB1348165D
申请日：1971-06-28
申请人： SANDOZ LTD
IPC分类号： C07D295/28 , C07D29/32 , A61K27/00 , C07C121/14 , C07D51/70
摘要： 1348165 N - [N - (cyanoalkyl) - N - nitroso]- amino-amino alcohol esters SANDOZ Ltd 28 June 1971 [30 June 1970 28 Aug 1970] 30124/71 Heading C2C Novel compounds of Formula I (in which each of R 1 and R 2 is H or C 1-4 alkyl, R 3 is -(R 5 )-CH 2 -X and R 4 is -(R 5 )-CH 3 or -(R 5 )-CH 2 -X, or R 3 and R 4 , together with the N atom, form a radical of Formula II or III in which R 5 is C 1-7 alkylene, X is -ONO 2 or -OCOR 6 , R 6 is C 1-4 alkyl optionally substituted by 1 to 3 F or Cl atoms, R 7 is C 1-3 alkylene, p is 4, 5 or 6 and q is 0 or 1, with the proviso that, in Formula III, when q is 0, the substituent is not on a carbon atom adjacent to the nitrogen atom), and pharmaceutically acceptable acid addition salts thereof, are prepared by (a) nitrating a corresponding compound I in which each X is OH and/or the nitroso group is absent, or (b) acylating a corresponding compound I in which each X is OH by reaction with an appropriate acid anhydride or halide, and, if desired, converting the free bases into acid addition salts. 4 - [N - (2 - cyanoisopropyl) - N - nitroso]- amino - 1 - piperazine - ethanol nitrate is prepared by reacting 4-amino-1-piperazine-ethanol with KCN followed by acetone to give 4-[N- (2 - cyanoisopropyl) - amino] - 1 - piperazineethanol and then nitrating this by treatment with a mixture of acetic anhydride and nitric acid. Pharmaceutical compositions having antianginal activity for oral administration comprise a compound I or a pharmaceutically acceptable acid addition salt thereof, together with a pharmaceutical carrier.

9. 发明专利

DE1670386A1 未知
公开(公告)号：DE1670386A1
公开(公告)日：1970-11-05
申请号：DE1670386
申请日：1966-09-20
申请人： CIBA GEIGY
发明人： RAYMOND BERNASCONI DR , KARL SCHENKER DR
IPC分类号： C07D295/155 , C07D29/32
摘要： 1,128,079. Cyclohexane derivatives. CIBA Ltd. 26 Sept., 1966 [29 Sept., 1965; 19 Aug., 1966], No. 42872/66. Heading C2C. Novel cyclohexane derivatives of the formula wherein X is an alkylene radical optionally interrupted by an oxygen atom, Ph is a phenyl radical which may be substituted by C 1-7 alkyl, hydroxyl, C 1-7 alkoxy ortrifluoromethyl radicals or by halogen atoms, and R is a cyano or carbalkoxy radical, and acid addition salts thereof are prepared (1) by condensing heterocyclic bases XN-H with the appropriate cyclohexanones R.PhC 6 H 8 O and reducing the cyclohexene derivatives RPhC 6 H 7 NX produced, (2) by reacting the bases XN-H with cyclohexane derivatives of the formula B.Ph.C 6 H 9 Z, where Z is a halogen atom or an arylsulphonyloxy radical, or (3) when R is carbalkoxy, by interconverting the corresponding cyano compound, e.g. by alcoholysis in the presence of sulphuric acid and ammonium chloride or by hydrolysing the cyano group to the carbamoyl group and hydrolysing the 1 -heterocyclyl - 4 - phenyl - 4 - carbamoyl-cyclohexanes produced to the corresponding 1 - heterocyclyl - 4 - phenyl - 4 - carboxycyclohexanes and esterifying these, e.g. with diazoalkanes, and, if desired, converting the free bases produced to the corresponding acid addition salts with inorganic or organic acids. The products of these processes may be cis- or (rans-forms or mixtures thereof, in which case the individual isomers may be isolated by conventional procedures, e.g. chromatography or fractional crystallization. 1 - Cyano - 1 - phenyl - 4 - (p - toluene - sulphonyloxy) - cyclohexane used as a starting material is prepared by reducing 4-cyano-4-phenylcyclohexanone with hydrogen or sodium borohydride and treating the 4-cyano-4-phenylcyclohexanol produced with p-toluenesulphonyl chloride. Therapeutic compositions useful as antitussives or analgesics contain compounds of the above formula or physiologically tolerable acid addition salts thereof, as active ingredient. The composition may be in a form suitable for enteral, parenteral or topical application.

10. 发明专利

AU6004073A FLUORESCENT BENZOFURAN COMPOUNDS 未知
公开(公告)号：AU6004073A
公开(公告)日：1975-03-06
申请号：AU6004073
申请日：1973-09-05
申请人： BASF AG
发明人： GRYCHTOL KLAUS
IPC分类号： C07D307/85 , C09B57/00 , C07D5/42 , C07C103/12 , B41M5/16 , C08K1/75 , C07C101/44 , C07D87/44 , C07D91/44 , C07D87/38 , C07D87/42 , C07D85/48 , C07D87/28 , C07D29/32 , C07D49/38 , C07D29/26 , C07D29/30 , C07D27/04 , C07D29/12
摘要： A benzofuran compound of the formula WHERE X denotes HSO4 , CH3SO4 , Cl , Br , 1/2 2ZnCl 4 or CH3COO . The said compounds are dyes for synthetic textile material.

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