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31. 发明申请

US20050209242A1 Theophylline and 3-isobutyl-1 methylxanthine based N-7 substituted derivatives displaying inhibitory activities on PDE-5 phospodiesterase 有权
标题翻译：茶碱和3-异丁基-1-甲基黄嘌呤的N-7取代衍生物显示对PDE-5磷酸二酯酶的抑制活性
公开(公告)号：US20050209242A1
公开(公告)日：2005-09-22
申请号：US11122343
申请日：2005-05-04
申请人： Ing-Jun Chen
发明人： Ing-Jun Chen
IPC分类号： A61K31/522 , C07D473/02 , C07D473/06 , C07D473/08
CPC分类号： C07D473/06 , C07D473/08
摘要： A variety of N-substituted derivatives based upon the base chemicals of that provide for the induction of cavernosal relaxation in animals.
摘要翻译：基于其的基础化学物质的各种N-取代衍生物提供用于诱导动物的海绵体松弛。

32. 发明申请

US20050009886A1 1,4-Dihydropyridine derivative with a guaiacoxypropanolamine and/or phenoxypropanolamine moiety 审中-公开
标题翻译： 1,4-二氢吡啶衍生物与愈创木酚丙酮胺和/或苯氧丙醇胺部分
公开(公告)号：US20050009886A1
公开(公告)日：2005-01-13
申请号：US10851293
申请日：2004-05-24
申请人： Ing-Jun Chen
发明人： Ing-Jun Chen
IPC分类号： C07D211/90 , A61K31/455 , C07D213/46
CPC分类号： C07D211/90
摘要： The invention pertains to a compound of the following formulas: wherein R1 and R3 are each individually selected from the group consisting of —X, —H, —NO2, CF3, saturated C1-C6 alkyl chain, unsaturated C2-C6 alkyl chain, saturated C1-C6 alkoxy chain, and unsaturated C2-C6 alkoxy chain, and wherein X represents a halogen. The inventive compounds exhibit pharmacological activity for blocking an α-, β-adrenoreceptor or calcium channel, inducing hypotension or inducing vaso-relaxation.
摘要翻译：本发明涉及下式的化合物：其中R 1和R 3各自独立地选自-X，-H，-NO 2，CF 3，饱和C 1 -C 6烷基链，不饱和C 2 -C 6烷基链，饱和 C1-C6烷氧基链和不饱和C2-C6烷氧基链，其中X表示卤素。本发明化合物表现出用于阻断α-，β-肾上腺素受体或钙通道，诱导低血压或诱导血管松弛的药理活性。

33. 发明授权

US06794399B2 1,4-dihydropyridine derivative with a guaiacoxypropanolamine and/or phenoxypropanolamine moiety 失效
标题翻译： 1,4-二氢吡啶衍生物与愈创木酚丙醇胺和/或苯氧基丙醇胺部分
公开(公告)号：US06794399B2
公开(公告)日：2004-09-21
申请号：US10119709
申请日：2002-04-11
申请人： Ing-Jun Chen
发明人： Ing-Jun Chen
IPC分类号： A61K314418
CPC分类号： C07D211/90
摘要： The invention disclosed some 1,4-dihydropiridine derivative chemically with guaiacoxypropanolamine based phenoxypropanolamine moiety and pharmacologically with &bgr;-adrenoceptor blocking and partial &bgr;2-agonist activities, is now emerging. The compound of 1,4-dihydropiridine derivative wherein has the formula I, wherein R selected from four group as follow R1 selected from X, H, NO2 saturated C1-C6 alkyl chain, unsaturated C6-C6 alkyl chain, R2 selected from H, CH3 R3 and R4 are individually selected from saturated C1-C6 alkyl chain, unsaturated C1-C6 alkyl chain; R5 selected from OH, saturated C1-C6 alkyl chain, unsaturated C1-C6 alkyl chain.
摘要翻译：本发明公开了一些以愈创木酚氧丙醇胺为基础的苯氧基丙胺胺部分化学发现的1,4-二氢吡啶衍生物，其药理学上具有β-肾上腺素能受体阻断和部分β2-激动剂活性。目前正在出现1,4-二氢嘧啶衍生物，其中式Ⅰ化合物，其中选自X，H，NO 2饱和C 1 -C 6烷基链，不饱和C 6 -C 6烷基链，选自H，CH 3 R 3和R 4的R 4的四个R中的R选自饱和C 1 -C 6烷基链，不饱和C 1 -C 6烷基链， C6烷基链; R5选自OH，饱和C1-C6烷基链，不饱和C1-C6烷基链。

34. 发明授权

US5939578A Vasomolol: an ultra short-acting and vasodilatory vanilloid type .beta..sub. - adrenoceptor antagonist 失效
标题翻译： Vasomolol：超短效和血管扩张性香草素型β1-肾上腺素受体拮抗剂
公开(公告)号：US5939578A
公开(公告)日：1999-08-17
申请号：US667648
申请日：1996-06-21
申请人： Ing-Jun Chen
发明人： Ing-Jun Chen
IPC分类号： C07C213/04 , C07C217/36
CPC分类号： C07C213/04
摘要： This invention is related to novel vasomolol, compounds of this invention have the following formula wherein R.sub.1 represents C.sub.1-4 alkyl group. ##STR1## vasomolol is an ultra short-acting and vasodilatory selective .beta..sub.1 -adrenoceptor antagonist, and is devoid of ISA.Vasomolol is an utra short acting and vasodilatory selective .beta..sub.1 -adrenoceptor antagonist, and is devoid of IA. The ultra short-acting and vsodilatory .beta..sub.1 -adrenoceptor blocking activities of vasomolol-a guaiacoxypropanolamine derivative of vanillic acid ethyl ester--were studied. Vasomolol (0.5, 1.0, 3.0 mg/kg, I.v.) produced a dose-dependent bradycardia rsponse, and particularly a hypotensive action with an ultra short-acting property in pentobarbital-anesthetized normotensive rats. Vasomolol's steady-state of .beta.-blockade was attained within 10 min after initiation of an infuson and a rapid recovery from blockade took place after termination of the infusion. In isolated rat aorta, vasomolol (10.sup.-6 M-10.sup.-5 M) inhibit both henylephrine (10.sup.-6 M) and High K.sup.+ (75 mM)--induced smooth muscle contractions, concentration-dependently. This inhibitory effect of vasomolol was more sensitive on K.sup.+ than on phenylephrine-induced contractions.
摘要翻译：本发明涉及新型血管舒洛尔，本发明化合物具有下式，其中R 1表示C 1-4烷基。血管舒缩是一种超短效和血管扩张性选择性β1-肾上腺素受体拮抗剂，没有ISA。 Vasomolol是一种utra短作用和血管扩张选择性β1-肾上腺素受体拮抗剂，没有IA。研究了vasomolol-一种香草酸乙酯的愈创木酚氧丙醇胺衍生物的超短效和降脂β1-肾上腺素受体阻断活性。 Vasomolol（0.5,1.0,3.0mg / kg，I.v。）产生剂量依赖性心动过缓反应，特别是在戊巴比妥麻醉的血压正常的大鼠中具有超短效性的降血压作用。 Vasomolol的稳定状态的β-阻断在开始信号后10分钟内达到，并且在输注终止后发生封锁的快速恢复。在分离的大鼠主动脉中，血管舒缓（10-6M-10-5M）抑制肾上腺素（10-6M）和高K +（75mM）诱导的平滑肌收缩，浓度依赖性。血管舒缓的这种抑制作用对K +比对去氧肾上腺素诱导的收缩更敏感。

35. 发明授权

US5804603A Synthesized .beta.-adrenergic blockers derivatives of guaiacol 失效
标题翻译：愈创木酚的合成β-肾上腺素能阻滞剂衍生物
公开(公告)号：US5804603A
公开(公告)日：1998-09-08
申请号：US559208
申请日：1995-11-13
申请人： Ing-Jun Chen
发明人： Ing-Jun Chen
IPC分类号： C07C45/74 , C07C225/16 , C07C233/25 , C07D295/092 , A61K31/165 , C07C233/05
CPC分类号： C07D295/088 , C07C225/16 , C07C233/25 , C07C45/74
摘要： Compounds of formula I ##STR1## in which OR.sup.1 is --OR.sub.3 NR.sub.4, in which R3 is a secondary alcohol group with 1.0 to 6 carbon atoms; a cyclic oxygen containing group with two carbon atoms; a pyridylmethyl or a piperidyl-ethyl group, R.sub.2 is alkyl, an ester group, an aldehyde group, a carboxylic acid group or a ketone group with 3 to 6 carbon --O--CONHR.sub.9 atoms, the group O--R.sub.7 NCOR.sub.8 or the group --O--CONHR.sub.9 in which R.sub.4 is an alkyl group with 1 to 8 carbon atoms, R.sub.7 is an alkylene group with 1 to 6 carbon atoms, each of R.sub.8 and R9 is an alkyl group with 1 to 12 carbon atoms and their pharmaceutically acceptable acid addition salts, are selective .beta.-blockers, antagonists of platelet aggregation, and .beta.-receptor binding. The processes of preparation, compositions, method of treatment are also described.
摘要翻译：其中OR 1为-OR 3 NR 4的式I的化合物，其中R 3为具有1.0至6个碳原子的仲醇基; 具有两个碳原子的含环氧基团; 吡啶基甲基或哌啶基乙基，R 2为烷基，酯基，醛基，羧酸基或具有3〜6个碳-O-CONHR 9原子的酮基，O-R7NCOR8或-O -CONHR 9，其中R 4是具有1至8个碳原子的烷基，R 7是具有1至6个碳原子的亚烷基，R 8和R 9各自是具有1至12个碳原子的烷基及其药学上可接受的酸加成盐是选择性β-阻滞剂，血小板聚集拮抗剂和β-受体结合。还描述了制备方法，组合物，治疗方法。

36. 发明授权

US08497370B2 Processes for preparing amine salts of sildenafil-analogues and use thereof 有权
标题翻译：制备西地那非类似物的胺盐的方法及其用途
公开(公告)号：US08497370B2
公开(公告)日：2013-07-30
申请号：US13044899
申请日：2011-03-10
申请人： Ing-Jun Chen
发明人： Ing-Jun Chen
IPC分类号： C07D473/00 , A61K31/497 , C08B15/06
CPC分类号： A61K31/519 , C07D487/04 , C08L1/286 , C08L5/00
摘要： A series of amine salts including a structure of formula (I) and formula (III) have provided. In formula I or formula (III), R1, Ra and RX are as defined in the specification. The amine complex salts disclosed in the present invention are characterized in a pro-drug active form and various pharmaceutical function.
摘要翻译：提供了包括式（I）和式（III）的结构的一系列胺盐。在式I或式（III）中，R 1，R a和R RX如说明书中所定义。本发明公开的胺络盐的特征在于前药活性形式和各种药物功能。

37. 发明申请

US20120095013A1 USE OF KMUP-3 FOR MYOCARDIAL INFARCTION 审中-公开
标题翻译：使用KMUP-3用于心肌梗塞
公开(公告)号：US20120095013A1
公开(公告)日：2012-04-19
申请号：US13085017
申请日：2011-04-12
申请人： Ing-Jun Chen
发明人： Ing-Jun Chen
IPC分类号： A61K31/522 , A61P9/10 , C07D473/08
CPC分类号： C07D473/08 , A61K31/522
摘要： A pharmaceutical composition for improving a cardiac function is provided. The pharmaceutical composition comprises an effective amount of an active component being one of a KMUP-3 compound and a salt thereof.
摘要翻译：提供了用于改善心脏功能的药物组合物。药物组合物包含有效量的作为KMUP-3化合物及其盐之一的活性成分。

38. 发明申请

US20110201618A1 KMUPS INHIBITING PROLIFERATION AND OBLITERATION OF PULMONARY ARTERY 审中-公开
标题翻译： KMUPS抑制肺动脉高压和排斥
公开(公告)号：US20110201618A1
公开(公告)日：2011-08-18
申请号：US13095393
申请日：2011-04-27
申请人： Ing-Jun CHEN
发明人： Ing-Jun CHEN
IPC分类号： A61K31/496 , A61P11/00
CPC分类号： A61K31/522
摘要： An obstructive pulmonary disease inhibiting pharmaceutical composition is provided. The obstructive pulmonary disease inhibiting pharmaceutical composition includes: an effective amount of a compound of formula I, wherein R2 and R4 are each selected independently from the group consisting of a C1˜C5 alkoxy group, a hydrogen, a nitro group, and a halogen atom; and a pharmaceutically acceptable carrier.
摘要翻译：提供阻塞性肺疾病抑制药物组合物。阻塞性肺疾病抑制药物组合物包括：有效量的式I化合物，其中R 2和R 4各自独立地选自C 1 -C 5烷氧基，氢，硝基和卤素原子 ; 和药学上可接受的载体。

39. 发明申请

US20100022552A1 KMUP-1 CAPABLE OF TREATING HYPERTENSION 审中-公开
标题翻译： KMUP-1可处理高血压
公开(公告)号：US20100022552A1
公开(公告)日：2010-01-28
申请号：US12572519
申请日：2009-10-02
申请人： Ing-Jun CHEN
发明人： Ing-Jun CHEN
IPC分类号： A61K31/496 , A61P9/12 , A61P9/00
CPC分类号： A61K31/522
摘要： A method for treating a spontaneous hypertension or a cardiomyocyte hypertrophy is provided. The method comprises a step of administering to a mammal a therapeutically effective amount of a compound of 7-[2-[4-(2-chlorobenzene)piperazinyl]ethyl]-1,3-dimethyl xanthine.
摘要翻译：提供了治疗自发性高血压或心肌细胞肥大的方法。该方法包括向哺乳动物施用治疗有效量的7- [2- [4-（2-氯苯）哌嗪基]乙基] -1,3-二甲基黄嘌呤化合物的步骤。

40. 发明申请

US20090209560A1 ANTI-INFLAMMATION ACTIVITY OF NEWLY SYNTHESIZED XANTHINE DERIVATIVES KMUP-1 AND KMUP-3 审中-公开
标题翻译：新合成的Xanthine衍生物KMUP-1和KMUP-3的抗炎活性
公开(公告)号：US20090209560A1
公开(公告)日：2009-08-20
申请号：US12429240
申请日：2009-04-24
申请人： Ing-Jun Chen , Bin-Nan Wu , Jwu-Lai Yeh
发明人： Ing-Jun Chen , Bin-Nan Wu , Jwu-Lai Yeh
IPC分类号： C12N5/06 , A61K31/52
CPC分类号： C07D473/08 , A61K31/522
摘要： An anti-inflammation substrate for decreasing the proinflammation induced by the cytokines and inhibiting the lung function degeneration is provided. The anti-inflammation substrate includes one selected from the group consisting of a 7-[2-[4-(2-chlorobenzene)piperazinyl]ethyl]-1,3-dimethylxanthine, a 7-[2-[4-(4-nitrobenzene)piperazinyl]ethyl]-1,3-dimethylxanthine, a respective pharmaceutical acceptable salt thereof, and a combination thereof.
摘要翻译：提供了用于降低由细胞因子诱导的促炎症并抑制肺功能退化的抗炎底物。抗炎底物包括选自7- [2- [4-（2-氯苯）哌嗪基]乙基] -1,3-二甲基黄嘌呤，7- [2- [4-（4- 硝基苯）哌嗪基]乙基] -1,3-二甲基黄嘌呤，其各自的药学上可接受的盐及其组合。

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