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1. 发明授权

US3895017A 3-Acetyl-1-alkyl-1,4-dihydro-4-oxo-1,8-naphthyridines and intermediates 失效
标题翻译： 3-乙酰基-1-烷基-1,4-二氢-4-氧代-1,8-萘啶和中间体
公开(公告)号：US3895017A
公开(公告)日：1975-07-15
申请号：US45392874
申请日：1974-03-22
申请人： STERLING DRUG INC
发明人： LESHER GEORGE Y , BRUNDAGE RUTH PAULINE
IPC分类号： C07D471/04 , C07D31/36
CPC分类号： C07D471/04
摘要： Process of reacting 2-amino-6-Q''-pyridine (I) with lower-alkyl (lower-alkoxy)methyleneacetoacetate (II) to produce lower-alkyl Alpha -(6-Q''-2-pyridylaminomethylene)acetoacetate (III''), heating lower-alkyl Alpha -(6-Q-2-pyridylaminomethylene)acetoacetate (III), to produce 3-acetyl-1,4-dihydro-7-Q-4-oxo-1,8naphthyridine (IV) which is tautomeric with 3-acetyl-4-hydroxy-7Q-1,8-naphthyridine (IVA), reacting IV (or IVA) with a loweralkylating agent to produce 3-acetyl-1-(lower-alkyl)-1,4-dihydro7-Q-4-oxo-1,8-naphthyridine (V) and converting V to 1-(loweralkyl)-1,4-dihydro-7-Q-4-oxo-1,8-naphthyridine-3-carboxylic acid (VI), where Q is lower-alkyl, hydroxymethyl, loweralkanoyloxymethyl, 4(or 3)-pyridyl or 4(or 3)-pyridyl having one or two lower-alkyl substituents, and Q'' is like Q but excluding lower-alkanoyloxymethyl. The compounds of formula VI are known antibacterial agents. Also given are alternative routes of preparing III and IV where Q is lower-alkanoyloxymethyl by reacting the N-oxides of III and IV, respectively, where Q is methyl with a lower-alkanoic acid anhydride.
摘要翻译：使2-氨基-6-Q'-吡啶（I）与低级烷基（低级烷氧基）亚甲基乙酰乙酸酯（II）反应生成低级烷基α-（6-Q'-2-吡啶基氨基亚甲基）乙酰乙酸酯（III' ），加热低级烷基α-（6-Q-2-吡啶基氨基亚甲基）乙酰乙酸酯（III），得到3-乙酰基-1,4-二氢-7-Q-4-氧代-1,8-萘啶（IV）其与3-乙酰基-4-羟基-7-Q-1,8-二氮杂萘（IVA）是互变异构体，使IV（或IVA）与低级烷基化剂反应以产生3-乙酰基-1-（低级烷基） -1,4-二氢-7-Q-4-氧代-1,8-二氮杂萘（V）并将V转化为1-（低级烷基）-1,4-二氢-7-Q-4-氧代-1 （VI），其中Q是具有一个或两个低级烷基取代基的低级烷基，羟甲基，低级烷酰氧基甲基，4（或3） - 吡啶基或4（或3） - 吡啶基， Q'如Q，但不包括低级烷酰氧基甲基。式VI化合物是已知的抗菌剂。还给出了制备III和IV的替代途径，其中Q是低级烷酰氧基甲基，分别通过使III和IV的N-氧化物与低级链烷酸酐反应。

2. 发明授权

US3884928A Imidazole derivatives 失效
标题翻译：咪唑衍生物
公开(公告)号：US3884928A
公开(公告)日：1975-05-20
申请号：US45453774
申请日：1974-03-25
申请人： HOFFMANN LA ROCHE
发明人： BRUDERER HANS , RUEGG RUDOLF
IPC分类号： C07D233/54 , C07D233/90 , C07D401/12 , C07D31/36 , C07D49/36
CPC分类号： C07D233/90 , Y10S514/962
摘要： Imidazole derivatives of the formula

WHEREIN R1, R2 and R4 are as hereinafter mentioned, are described. The imidazole derivatives are useful as psychosedative and analgesic agents.
摘要翻译：描述了式WHEREIN R1，R2和R4的咪唑衍生物如下文所述。咪唑衍生物可用作精神和镇痛剂。

3. 发明授权

US3835146A Substituted fusaric acid derivatives 失效
标题翻译：取代的富马酸衍生物
公开(公告)号：US3835146A
公开(公告)日：1974-09-10
申请号：US25783472
申请日：1972-05-30
申请人： BANYU PHARMA CO LTD , HIDAKA HIROYOSHI
发明人： MIYANO T , SUZUKI K , FUKATSU H
IPC分类号： C07D213/79 , C07D213/81 , C07D31/36
CPC分类号： C07D213/79 , C07D213/81
摘要： Halo-fusaric acid derivatives of the formula:

WHEREIN X represents halogen or hydrogen, Y represents halogen, and Z represents - OM or an amine, wherein M represents hydrogen or a salt or ester residue thereof which are characterized by significant activity in inhibiting the formation of dopamineBeta -hydroxylase and in the treatment of hypertension, and which are further characterized by relatively low toxicity, are prepared by reacting dehydrofusaric acid with a halogen or a hydrogen halide. Alternatively, these compounds can be produced by reacting halo-fusaric acid with an acyloxhalomethyl ester.
摘要翻译：下式的卤代糠酸衍生物：

4. 发明授权

US3830821A Pyridoxal alpha-ketoglutarate and pyridoxamine alpha-ketoglutarate 失效
标题翻译：吡咯烷酮 - 乙酸丁酯和吡咯烷酮ALPHA-KETOGLUTARATE
公开(公告)号：US3830821A
公开(公告)日：1974-08-20
申请号：US29605672
申请日：1972-10-10
申请人： MADE LABOR SA
发明人： ROLDAN C , FERNANDEZ M
IPC分类号： C07D213/66 , C07D31/36
CPC分类号： C07D213/66
摘要： PYRIDOXAL ALPHA-KETOGLUTARATE AND PYRIDOXAMINE ALPHAKETOGLUTRATE POSSESS ANTI-CONVULSANT, WEIGHT INCREASE AND ANTI-HYPNOTIC PROPERTIES.

5. 发明授权

US3799936A Unsymmetrical esters of 1,4-dihydropyridine 3,5-dicarboxylates 失效
标题翻译： 1,4-二羟基吡啶3,5-二异氰酸酯的非对称酯
公开(公告)号：US3799936A
公开(公告)日：1974-03-26
申请号：US24223872
申请日：1972-04-07
申请人： BAYER AG
发明人： MEYER H , BOSSERT F , VATER W , STOEPEL K
IPC分类号： A61K31/455 , C07D211/90 , C07D31/36
CPC分类号： A61K31/455 , C07D211/90
摘要： UNSYMMERTICAL ESTERS OF 4-SUBSTITUTED - 1,4 - DIHYDROPYRIDINE 3,5 - DICARBOXYLIC ACID OPTIONALLY SUBSTITUTED BY LOWER ALKYL GROUPS IN THE 2- AND 6-POSITIONS ARE CARDIOVASCULAR AGENTS. THE COMPOUNDS, OF WHICH 2,6-DIMETHYL4 - (2'' - METHYL PHENYL) - 1,4 - DIHYDROPYRIDINE 3,5-DICARBOXYLIC ACID 3-METHYL-5-ALLYL ESTER IS A TYPICAL EXAMPLE, CAN BE PREPARED THROUGH CONDENSATION OF AN YLIDENE-BKETOCARBOXYLIC ACID ESTER WITH EITHER AN ENAMINO CARBOXYLIC ACID ESTER OR A B-KETOCARBOXYLIC ACID ESTER AN AMMONIA.

6. 发明授权

US3786043A 7-methyl-4-chloro (or -4-lower-alkoxy)-1,8-naphthyridine-3-carboxylates 失效
标题翻译： 7-甲基-4-氯代（或4-低级 - 烷基）-1,8-萘基-3-羧酸酯
公开(公告)号：US3786043A
公开(公告)日：1974-01-15
申请号：US3786043D
申请日：1972-06-19
申请人： STERLING DRUG INC
发明人： BRUNDAGE R , LESHER G
IPC分类号： C07D471/04 , C07D31/36
CPC分类号： C07D471/04
摘要： LOWER-ALKYL 4 - Q - 7 METHYL-1,8-NAPHTHYRIDINE-3CARBOXYLATES (1) WHERE Q IS CHLORO OR LOWER-ALKOXY ARE PREPARED BY REACTING LOWER-ALKYL 1,4-DIHYDRO-7-METHYL-4OXO - 1,8 - NAPHTHYRIDINE - 3 - CARBOXYLATE (II) WITH A CHLORINATING AGENT TO PRODUCE SAID 4-CHLORO COMPOUND (IA) WHICH BY REACTION WITH ALKALI METAL LOWER-ALKOXIDE, PREFERABLY USING LOWER-ALKANOL AS SOLVENT, PRODUCES SAID 4-(LOWER-ALKOXY) COMPOUND (IB). SAID 4-CHLORO COMPOUND WHEN HEATED WITH ALKALI METAL LOWER-ALKOXIDE OR SAID 4-(LOWER-ALKOXY) COMPOUND WHEN HEATED YIELD THE KNOWN ANTIBACTERIALLY ACTIVE LOWER-ALKYL 1-(LOWER-ALKYL)1,4 - DIHYDRO - 7 - METHYL - 4 - OXO-1,8-NAPHTHYRIDINE-3CARBOXYLATES.

7. 发明授权

US3755340A Amino derivatives of pyrazolopyridine carboxylic acids and esters 失效
标题翻译：吡唑并吡啶羧酸和酯的氨基衍生物
公开(公告)号：US3755340A
公开(公告)日：1973-08-28
申请号：US3755340D
申请日：1971-08-05
申请人： HOEHN H , DENZEL T
发明人： HOEHN H , DENZEL T
IPC分类号： A61K31/435 , A61P25/00 , A61P25/04 , A61P25/20 , A61P29/00 , C07D213/80 , C07D231/38 , C07D261/14 , C07D401/06 , C07D405/06 , C07D471/04 , C07D498/04 , C07D31/36
CPC分类号： C07D213/80 , C07D231/38 , C07D261/14 , C07D471/04
摘要： New amino derivatives of pyrazolo(3,4-b)pyridine-5-carboxylic acids and esters have the general formula

THEY ARE USEFUL AS ATARACTIC, ANALGESIC AND ANTIINFLAMMATORY AGENTS. In addition, the new compounds increase the intracellular concentration of adenosine-3'',5''-cyclic monophosphate.
摘要翻译：吡唑并[3,4-b]吡啶-5-羧酸和酯的新氨基衍生物具有通用作为药物，毒理和抗炎药物的通式。此外，新化合物增加了腺苷-3'，5'-环状单磷酸的细胞内浓度。

8. 发明授权

US3752819A 5-phenyl-isoxazole-3-carboxylic acids and their derivatives 失效
标题翻译： 5-苯基 - 异恶唑-3-羧酸及其衍生物
公开(公告)号：US3752819A
公开(公告)日：1973-08-14
申请号：US3752819D
申请日：1970-12-02
申请人： FERLUX
发明人： PHILIPPE J
IPC分类号： C07D295/02 , C07C59/90 , C07D261/18 , C07D311/24 , C07D31/36
CPC分类号： C07D311/24 , C07C59/90 , C07D261/18 , Y10S514/869
摘要： NEW DERIVATIVES OF 5-PHENYL-ISOXAZOLE-3-CARBOXYLIC ACID OF THE GENERAL FORMULA

3-(R-CO-),5-(2-R1,3-R2,4-R3,5-R4,6-R5-PHENYL)-ISOXAZOLE

IN WHICH R REPRESENTS A FREE OR ESTERIFIED HYDROXYLATED GROUP, AN AMINATED GROUP OR HYDRAZINE GROUP, THESE DERIVATIVES ARE PREPARED BY THE ACTION OF HYDROXLAMINE OR BENZOYLPYRUVIC ACIDS. THERAPEUTICAL APPLICATION OF THE DERIVATIVES OF THE INVENTION PARTICULARLY AS SALIDIURETICS, SEDATIVES, ANALGESICS.

9. 发明授权

US3734920A Diquinolonopyridone 失效
标题翻译：二环戊二烯
公开(公告)号：US3734920A
公开(公告)日：1973-05-22
申请号：US3734920D
申请日：1970-11-25
申请人： DU PONT
发明人： CHEN C
IPC分类号： C09B57/00 , C07D31/36
CPC分类号： C09B57/00
摘要： A CLASS OF COMPOUNDS OF WHICH DIQUINOLONOPYRIDONE IS ILLUSTRATIVE, AND NEW AND USEFUL PIGMENTS FORMED THEREFROM LONG WITH A CLASS OF INTERMEDIATES OF WHICH DIMETHYL-3,5-DIANILINOCHELIDAMATE IS TYPICAL.

10. 发明授权

US3691181A Certain acyl derivatives of the antibiotic t-2636c 失效
标题翻译：抗生素T-2636C的某些ACYL衍生物
公开(公告)号：US3691181A
公开(公告)日：1972-09-12
申请号：US3691181D
申请日：1969-10-27
申请人： TAKEDA CHEMICAL INDUSTRIES LTD
发明人： KISHI TOYOKAZU , HARADA SETSUO , MIZUNO KOMEI , HIGASHIDE EIJI , SHIBATA MOTOO
IPC分类号： C07G11/00 , A61K35/74 , C07D493/08 , C07D31/36 , C07D7/06
CPC分类号： C07D493/08
摘要： Acyl derivatives of Antibiotic T-2636C useful for inhibiting the growth of Gram positive bacteria and being effective against strains resistant to Oleandomycin and Erythromycin, and method for production thereof.

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