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1. 发明授权

US4644004A Pyridynecarboxylic esters of dopamine and of its N-alkyl derivatives 失效
标题翻译：多巴胺及其N-烷基衍生物的吡啶并羧酸酯
公开(公告)号：US4644004A
公开(公告)日：1987-02-17
申请号：US699598
申请日：1985-02-08
申请人： Cesare Casagrande , Emilio Mussini , Vittorio Vecchietti
发明人： Cesare Casagrande , Emilio Mussini , Vittorio Vecchietti
IPC分类号： A61K31/4406 , A61K31/455 , A61P7/10 , A61P9/08 , A61P9/12 , A61P13/02 , A61P15/00 , C07D213/79 , C07D213/80 , C07D401/02 , A61K31/44
CPC分类号： C07D213/79 , C07D213/80
摘要： Pyridinecarboxylic esters of dopamine and of its N-alkyl derivatives, salts thereof with pharmaceutically acceptable organic or inorganic acids, process for preparing them and pharmaceutical compositions containing them which are particularly useful in the treatment of cardiovascular and renal disorders.
摘要翻译：多巴胺及其N-烷基衍生物的吡啶羧酸酯，其盐与药学上可接受的有机酸或无机酸，其制备方法和含有它们的药物组合物，其特别可用于治疗心血管和肾脏疾病。

2. 发明授权

US4528296A Derivatives of aminopyridinecarboxylic acids and pharmaceutical compositions containing them 失效
标题翻译：氨基吡啶羧酸的衍生物和含有它们的药物组合物
公开(公告)号：US4528296A
公开(公告)日：1985-07-09
申请号：US557584
申请日：1983-12-02
申请人： Vittorio Vecchietti , Giorgio Ferrari , Cesare Casagrande
发明人： Vittorio Vecchietti , Giorgio Ferrari , Cesare Casagrande
IPC分类号： C07D213/79 , C07D213/80 , A61K31/455 , C07D213/75
CPC分类号： C07D213/79
摘要： Derivatives of aminopyridinecarboxylic acids which inhibit the dipeptidyl carboxy peptidase (DPCP), methods for their preparation and pharmaceutical compositions containing them.The compounds have formula: ##STR1## where Z is hydrogen, alkyl having from 1 to 3 carbon atoms, halogen or alkoxy having from 1 to 3 carbon atoms;R1 is hydrogen, alkyl having from 1 to 6 carbon atoms, arylalkyl having from 7 to 12 carbon atoms, aryl having from 6 to 15 carbon atoms;m and n are an integer of from 0 to 4 each provided, however, the m+n is lower than 5;R2 is hydrogen, alkyl having from 1 to 6 carbon atoms or arylalkyl having from 7 to 12 carbon atoms;R3 is hydrogen or acyl having from 1 to 8 carbon atoms;R4 is hydrogen or alkyl having from 1 to 3 carbon atoms;and their pharmaceutically acceptable salts with organic or inorganic acids.
摘要翻译：抑制二肽基羧基肽酶（DPCP）的氨基吡啶羧酸的衍生物，其制备方法和含有它们的药物组合物。该化合物具有式：其中Z是氢，具有1至3个碳原子的烷基，卤素或具有1至3个碳原子的烷氧基的式（I） R1是氢，具有1至6个碳原子的烷基，具有7至12个碳原子的芳基烷基，具有6至15个碳原子的芳基; m和n分别为0〜4的整数，m + n小于5; R2是氢，具有1至6个碳原子的烷基或具有7至12个碳原子的芳烷基; R3是氢或具有1至8个碳原子的酰基; R4是氢或具有1至3个碳原子的烷基; 及其与有机或无机酸的药学上可接受的盐。

3. 发明授权

US5438047A Diphosphates of catecholamines and pharmaceutical compositions containing them 失效
标题翻译：儿茶酚胺的二磷酸盐和含有它们的药物组合物
公开(公告)号：US5438047A
公开(公告)日：1995-08-01
申请号：US204394
申请日：1994-03-28
申请人： Francesco Santangelo , Cesare Casagrande , Gabriele Norcini
发明人： Francesco Santangelo , Cesare Casagrande , Gabriele Norcini
IPC分类号： C07F9/12 , A61K31/66
CPC分类号： C07F9/12
摘要： Diphosphates of catecholamines having formula (I) wherein R, R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, R.sub.6, R.sub.7 and X have the meanings reported in the description, are useful in the therapy of cardiovascular and renal diseases. ##STR1##
摘要翻译：式（I）的儿茶酚胺的二磷酸盐其中R，R 1，R 2，R 3，R 4，R 5，R 6，R 7和X具有说明书中报道的含义，可用于治疗心血管和肾脏疾病。（一）

4. 发明授权

US5151414A Phenoxyethyl amine compounds active on the cardiovascular system 失效
标题翻译：活性在心脏血管系统上的羟基乙胺化合物
公开(公告)号：US5151414A
公开(公告)日：1992-09-29
申请号：US738608
申请日：1991-07-31
申请人： Cesare Casagrande , Gabriele Norcini , Francesco Santangelo , Claudio Semeraro
发明人： Cesare Casagrande , Gabriele Norcini , Francesco Santangelo , Claudio Semeraro
IPC分类号： A61K31/135 , A61K31/215 , A61K31/265 , A61K31/27 , A61K31/33 , A61K31/66 , A61P9/00 , A61P9/08 , A61P9/12 , A61P25/28 , C07C217/14 , C07C217/20 , C07C219/26 , C07C219/28 , C07C271/44 , C07D521/00 , C07F9/12
CPC分类号： C07C271/44 , C07C217/20 , C07F9/12 , C07C2102/10
摘要： Compounds of formula ##STR1## (wherein R, R.sub.1, R.sub.2, R.sub.3, n, m and p have the meanings reported in the specification), their preparation and the compositions for pharmaceutical use containing them as active ingredient are described.The compounds of formula I have dopaminergic vasodilator activity and they may be used in pharmaceutical field.

5. 发明授权

US4673671A Method for improving the absorption and effectiveness of a catecholamine compound 失效
标题翻译：用于改善儿茶酚胺化合物的吸收和有效性的方法
公开(公告)号：US4673671A
公开(公告)日：1987-06-16
申请号：US748587
申请日：1985-06-25
申请人： Cesare Casagrande , Francesco Santangelo
发明人： Cesare Casagrande , Francesco Santangelo
IPC分类号： A61K31/685 , A61P7/10 , A61P9/08 , A61P9/12 , A61P43/00 , C07F9/09 , C07F9/12 , C07F9/553 , C07F9/576 , C07F9/62 , A61K31/675
CPC分类号： C07F9/62 , C07F9/12 , C07F9/5532
摘要： A catecholamine compound is converted to a new mono O-phosphate ester derivative thereof which exhibit improved absorption and effectiveness.
摘要翻译：将儿茶酚胺化合物转化为新的单O-磷酸酯衍生物，其表现出改善的吸收和有效性。

6. 发明授权

US4302471A Method of treating cardiac and renal failures 失效
标题翻译：治疗心脏和肾衰竭的方法
公开(公告)号：US4302471A
公开(公告)日：1981-11-24
申请号：US151632
申请日：1980-05-20
申请人： Cesare Casagrande , Giorgio Ferrari
发明人： Cesare Casagrande , Giorgio Ferrari
IPC分类号： A61K31/22 , A61K20060101 , A61K31/21 , A61K31/215 , A61K31/24 , A61P9/00 , A61P9/04 , C07C20060101 , C07C211/00 , C07C217/00 , C07C219/28
CPC分类号： C07C46/00
摘要： The present invention relates to a method of inducing a response dopamine-like in an animal having impaired cardiovascular and renal functions, comprising administering to said animal an effective amount of a compound having the general formula: ##STR1## wherein R is a secondary or tertiary alkyl radical having from 3 to 7 carbon atoms, and their salts with nontoxic organic and inorganic acids.In particular, the present invention relates to a method of treating cardiac and renal failures comprising administering to a patient suffering therefrom an effective amount of a compound having the above-identified general formula, in suitable pharmaceutical preparations.
摘要翻译：本发明涉及在具有心血管和肾功能受损的动物中诱导多巴胺样反应的方法，其包括向所述动物施用有效量的具有以下通式的化合物：其中R是二级或三级具有3至7个碳原子的烷基，以及它们与无毒有机和无机酸的盐。特别地，本发明涉及治疗心脏和肾衰竭的方法，包括在合适的药物制剂中向患有其的患者施用有效量的具有上述通式的化合物。

7. 发明授权

US5144059A Catecholamine esters 失效
标题翻译：青蒿素酯
公开(公告)号：US5144059A
公开(公告)日：1992-09-01
申请号：US512212
申请日：1990-04-20
申请人： Cesare Casagrande , Francesco Santangelo
发明人： Cesare Casagrande , Francesco Santangelo
IPC分类号： A61K31/17 , A61K31/22 , A61K31/235 , A61K31/255 , A61P9/00 , A61P13/02 , A61P15/00 , A61P27/02 , C07C213/08 , C07C219/28 , C07C219/30 , C07C271/16 , C07C271/18 , C07C271/44 , C07C303/34 , C07C307/02
CPC分类号： C07C271/44 , C07C219/28 , C07C219/30 , C07C271/16 , C07C271/18 , C07C307/02
摘要： The compound of the formula ##STR1## (wherein R, R.sub.1 and R.sub.2 have the meanings given in the description), salts thereof with pharmaceutically acceptable organic or inorganic acids, process and intermediates for the preparation thereof and a pharmaceutical composition containing said compound are described.The compounds of formula I and the salts thereof are useful in the treatment of heart and renal diseases.

8. 发明授权

US5013753A Prodrugs of dopamine 失效
标题翻译：多巴胺的前药
公开(公告)号：US5013753A
公开(公告)日：1991-05-07
申请号：US386106
申请日：1989-07-28
申请人： Cesare Casagrande , Francesco Santangelo
发明人： Cesare Casagrande , Francesco Santangelo
IPC分类号： A61K31/195 , A61K31/198 , A61K31/22 , A61K31/24 , A61K31/33 , A61P9/00 , A61P25/00 , A61P43/00 , C07C237/12 , C07C237/22 , C07C239/06 , C07D213/79 , C07D521/00
CPC分类号： C07C237/12 , C07C237/22
摘要： Compounds of formula ##STR1## (wherein R, R.sub.1, R.sub.2 and X have the meanings reported in the specification), the processes for their preparation and the pharmaceutical compositions containing them as active ingredient are described.The compounds of formula I are useful in the treatment of Parkinson's disease, renal failure, cardiac decompensation and hypertension.

9. 发明授权

US4940800A Beazimidazole compounds active as inhibitors of the cholesterol biosynthesis 失效
标题翻译：活性为胆固醇生物合成抑制剂的比唑咪唑化合物
公开(公告)号：US4940800A
公开(公告)日：1990-07-10
申请号：US385369
申请日：1989-07-27
申请人： Giorgio Bertolini , Cesare Casagrande , Francesco Santangelo
发明人： Giorgio Bertolini , Cesare Casagrande , Francesco Santangelo
IPC分类号： C07D235/06 , A61K31/415 , A61K31/4184 , A61P3/06 , C07D235/18 , C07D235/24 , C07D405/06 , C07F7/18
CPC分类号： C07F7/1852 , C07D405/06
摘要： The compounds of formula ##STR1## wherein R, R.sub.1, R.sub.2, R.sub.3, and R.sub.4 have the meanings given in the specification, are described.The compounds of formula I are active as inhibitors of the enzyme HMG-CoA reductase and can be used in therapy as anti-hypercholesterolemics.

10. 发明授权

US4508719A Hydroxyimino and alkoxyimino derivatives of 1,4-dihydropyridine and anti-hypertensive compositions 失效
标题翻译： 1,4-二氢吡啶和抗高血压组合物的羟基亚氨基和烷氧基亚氨基衍生物
公开(公告)号：US4508719A
公开(公告)日：1985-04-02
申请号：US498248
申请日：1983-05-26
申请人： Silvia Z. Tricerri , Cesare Casagrande , Franco De Marchi , Massimo Nicola
发明人： Silvia Z. Tricerri , Cesare Casagrande , Franco De Marchi , Massimo Nicola
IPC分类号： C07D209/48 , C07D211/90 , A61K31/535 , A61K31/455 , C07D211/82 , C07D413/12
CPC分类号： C07D209/48 , C07D211/90
摘要： Compounds of formula I: ##STR1## are described in which R.sup.1 is a linear or branched alkyl radical containing between 1 and 5 carbon atoms, the alkyl radical being unsubstituted or substituted by an alkoxy group; R.sup.2 is an unsubstituted phenyl of phenyl substituted by a nitro group; R.sup.3 is hydrogen or a linear or branched alkyl residue containing between 1 and 4 carbon atoms, the alkyl radical being unsubstituted or substituted by at least one alkoxy or fluorine atom or both alkoxy and fluorine atoms; R.sup.4 is hydrogen or a linear or branched alkyl containing between 1 and 4 carbon atoms, the alkyl radical being unsubstituted or substituted by alkoxy, carbalkoxy, dialkylamino, 1-aryl or 1-heteroarylpiperazinyl, aryl or a monocyclic 5 or 6 membered heterocycle in which at least one of the heteroatoms is N,O,S such as 1-piperidinyl, 4-morpholinyl or R.sub.4 is alkenyl or cyclo(C.sub.3 -C.sub.6)alkyl; and enantiomers, racemates, diastereoisomers and isomers (E) and (Z) and their salts with pharmaceutically acceptable acids.The novel compounds exhibit calcium-antagonistic activity.
摘要翻译：描述了式I化合物：其中R 1是含有1至5个碳原子的直链或支链烷基，该烷基是未取代的或被一个烷氧基取代; R2是被硝基取代的苯基的未取代的苯基; R3是氢或含有1至4个碳原子的直链或支链烷基，烷基是未取代的或被至少一个烷氧基或氟原子或烷氧基和氟原子所取代; R4是氢或含有1至4个碳原子的直链或支链烷基，该烷基是未取代的或被烷氧基，烷氧基，二烷基氨基，1-芳基或1-杂芳基哌嗪基，芳基或单环5或6元杂环取代，其中至少一个杂原子是N，O，S如1-哌啶基，4-吗啉基或R4是烯基或环（C 3 -C 6）烷基; 和对映异构体，外消旋体，非对映异构体和异构体（E）和（Z）及其与药学上可接受的酸的盐。新化合物显示钙拮抗活性。

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