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1. 发明申请

US20160193160A1 Styrenyl Derivative Compounds for Treating Ophthalmic Diseases and Disorders 审中-公开
公开(公告)号：US20160193160A1
公开(公告)日：2016-07-07
申请号：US15072250
申请日：2016-03-16
申请人： Acucela Inc.
发明人： Ian Leslie Scott , Vladimir Aleksandrovich Kuksa , Anna Gall , Mark W. Orme , Jennifer Gage , Thomas L. Little, JR. , Qin Jiang , Lana Michele Rossiter , Kevin F. McGee , Ryo Kubota
IPC分类号： A61K31/137
CPC分类号： A61K31/5375 , A61K31/137 , A61K31/145 , A61K31/167 , A61K31/40 , A61K31/4453 , A61K31/495 , C07C211/27 , C07C211/28 , C07C211/29 , C07C215/08 , C07C215/30 , C07C215/42 , C07C215/46 , C07C217/10 , C07C217/16 , C07C217/18 , C07C217/48 , C07C217/54 , C07C217/62 , C07C217/72 , C07C225/06 , C07C225/18 , C07C233/05 , C07C237/04 , C07C317/28 , C07C323/25 , C07C323/32 , C07C323/33 , C07C2602/14 , C07C2602/16 , C07D207/06 , C07D211/14 , C07D295/03
摘要： The present invention relates generally to compositions and methods for treating neurodegenerative diseases and disorders, particularly ophthalmic diseases and disorders. Provided herein are styrenyl derivative compounds, including but not limited to stilbene derivative compounds, and compositions comprising these compounds, that are useful for treating and preventing ophthalmic diseases and disorders, including age-related macular degeneration (AMD) and Stargardt's Disease.

2. 发明申请

US20140323527A1 ARYLOXY AMINE COMPOUNDS AND THEIR USE AS SODIUM CHANNEL MODULATORS 审中-公开
标题翻译： ARYLOXY AMINE化合物及其作为钠通道调节剂
公开(公告)号：US20140323527A1
公开(公告)日：2014-10-30
申请号：US14222854
申请日：2014-03-24
申请人： Bevyn JARROTT
发明人： Bevyn JARROTT
IPC分类号： C07C217/58 , C07D213/68
CPC分类号： C07C217/58 , C07C217/16 , C07C217/18 , C07C217/20 , C07D213/68 , C07D231/22
摘要： The present invention relates generally to the field of therapeutic treatment and compounds having utility therefor, in particular the therapy or management of conditions associated with excessive, unwanted or undesirable sodium ion passage through cellular membranes via voltage-gated sodium channels. In one embodiment the invention is concerned with the treatment of neuropathic pain. The invention contemplates to aryloxy-substituted amines, as sodium channel blockers or modulators. In further embodiments, the invention also relates to compounds which may advantageously have dual sodium channel blocker/modulating and antioxidative (free-radical scavenging) effects. Methods for their manufacture and compositions containing the compounds are also contemplated.
摘要翻译：本发明一般涉及治疗性治疗领域和其用途的化合物，特别是治疗或管理与通过电压门控钠通道通过细胞膜的过量，不期望或不期望的钠离子相关的病症。在一个实施方案中，本发明涉及神经性疼痛的治疗。本发明考虑到作为钠通道阻断剂或调节剂的芳氧基取代的胺。在另外的实施方案中，本发明还涉及可有利地具有双钠通道阻断剂/调节和抗氧化（自由基清除）作用的化合物。也考虑了其制造方法和含有这些化合物的组合物。

3. 发明授权

US08633251B2 Derivatives of aminoalkanols, method of obtaining of aminoalkanols and their use 有权
标题翻译：氨基链烷醇的衍生物，获得氨基链烷醇的方法及其用途
公开(公告)号：US08633251B2
公开(公告)日：2014-01-21
申请号：US12863881
申请日：2009-01-19
申请人： Henryk Marona , Anna Waszkielewicz , Katarzyna Kiec-Kononowicz
发明人： Henryk Marona , Anna Waszkielewicz , Katarzyna Kiec-Kononowicz
IPC分类号： A61K31/135 , C07C213/00 , C07C215/00 , C07C217/00
CPC分类号： C07C217/18 , C07B2200/07 , C07C217/16 , C07C217/20 , C07C235/20 , C07C235/22 , C07C237/22 , C07C2601/14
摘要： The subject of the invention is a group of new derivatives of aminoalkanols, more specifically [(phenoxy)alkyl]aminoalkanols and [(phenoxy)acyl)aminoalkanols, their method of obtaining and their use for production of a medicine which is used in the prophylaxis, prevention and/or treatment of diseases or symptoms having neurological background and for production of a medicine with anticonvulsant activity, which is used in seizures of various origin, also in the limbic system, in myoclonic or sound-induced seizures, in psychomotor epilepsy, as well as in relieving neuropathic or inflammatory pain.
摘要翻译：本发明的主题是一组氨基链烷醇的新衍生物，更具体地是[（苯氧基）烷基]氨基链烷醇和[（苯氧基）酰基）氨基链烷醇的新衍生物，它们的获得方法及其用于生产用于预防的药物预防和/或治疗具有神经背景的疾病或症状，以及用于产生具有抗惊厥活性的药物，其用于各种起源的癫痫发作，也用于边缘系统，肌阵挛或声音诱发的癫痫发作，精神运动性癫痫，以及缓解神经性或炎性疼痛。

4. 发明申请

US20130289118A1 DERIVATIVES OF AMINOALKANOLS, METHOD OF OBTAINING OF AMINOALKANOLS AND THEIR USE 有权
标题翻译：氨基烷醇的衍生物，获得氨基烷醇的方法及其用途
公开(公告)号：US20130289118A1
公开(公告)日：2013-10-31
申请号：US13853542
申请日：2013-03-29
申请人： Anna Waszkielewicz , Uniwersylet Jagiellonski
发明人： Henryk Marona , Anna Waszkielewicz , Katarzyna Kiec-Kononowicz
IPC分类号： C07C217/18 , C07C235/20
CPC分类号： C07C217/18 , C07B2200/07 , C07C217/16 , C07C217/20 , C07C235/20 , C07C235/22 , C07C237/22 , C07C2601/14
摘要： The subject of the invention is a group of new derivatives of aminoalkanols, more specifically [(phenoxy)alkyl]aminoalkanols and [(phenoxy)acyl]aminoalkanols, their method of obtaining and their use for production of a medicine which is used in the prophylaxis, prevention and/or treatment of diseases or symptoms having neurological background and for production a medicine with anticonvulsant activity, which is used in seizures of various origin, also in the limbic system, in myoclonic or sound-induced seizures, in psychomotor epilepsy, as well as relieving neuropathic or inflammatory pain.
摘要翻译：本发明的主题是一组氨基链烷醇的新衍生物，更具体地是[（苯氧基）烷基]氨基链烷醇和[（苯氧基）酰基]氨基链烷醇的衍生物，它们的获得方法和它们用于生产用于预防的药物，预防和/或治疗具有神经背景的疾病或症状并用于生产具有抗惊厥活性的药物，其用于各种起源的缉获，也用于边缘系统，肌阵挛或声音诱发的癫痫发作，精神运动性癫痫中，作为以及缓解神经性或炎性疼痛。

5. 发明申请

US20110281844A1 NON-IMIDAZOLE ALKYLAMINES AS HISTAMINE H3-RECEPTOR LIGANDS AND THEIR THERAPEUTIC APPLICATIONS 审中-公开
标题翻译：作为组胺H3受体配体的非咪唑烷基胺及其治疗应用
公开(公告)号：US20110281844A1
公开(公告)日：2011-11-17
申请号：US12968807
申请日：2010-12-15
申请人： Jean-Charles SCHWARTZ , Jean-Michel ARRANG , Monique GARBARG , Jeanne-Marie LECOMTE , Xavier LIGNEAU , Walter G. SCHUNACK , Holger STARK , Charon Robin GANELLIN , Fabien LEURQUIN , Elz Sigurd
发明人： Jean-Charles SCHWARTZ , Jean-Michel ARRANG , Monique GARBARG , Jeanne-Marie LECOMTE , Xavier LIGNEAU , Walter G. SCHUNACK , Holger STARK , Charon Robin GANELLIN , Fabien LEURQUIN , Elz Sigurd
IPC分类号： A61K31/445 , C07D265/30 , A61K31/5375 , C07D223/04 , A61K31/55 , A61P3/04 , A61P1/08 , A61P25/28 , A61P25/24 , A61P25/06 , A61P29/00 , A61P17/00 , A61P11/00 , A61P27/02 , A61P1/00 , A61P1/04 , A61P19/02 , C07D211/20
CPC分类号： C07D213/74 , A61K31/396 , A61K31/397 , A61K31/40 , A61K31/445 , A61K31/55 , C07B2200/07 , C07C217/16 , C07C217/20 , C07C217/22 , C07C251/48 , C07C255/54 , C07C2602/10 , C07D207/20 , C07D211/58 , C07D211/60 , C07D211/62 , C07D211/70 , C07D215/38 , C07D215/46 , C07D239/42 , C07D271/06 , C07D277/82 , C07D295/03 , C07D295/088 , C07D295/096 , C07D295/13 , C07D295/185
摘要： Use of a compound of formula (A), wherein: W is a residue which imparts antagonistic and/or agonistic activity at histamine H3-receptors when attached to an imidazole ring in 4(5) position; R1 and R2 may be identical or different and represent each independently a lower alkyl or cycloalkyl, or taken together with the nitrogen atom to which they are attached, a saturated nitrogen-containing ring (i) as defined, a non-aromatic unsaturated nitrogen-containing ring (ii) as defined, a morpholino group, or a N-substituted piperazino group as defined for preparing medicaments acting as antagonists and/or agonists at the H3-receptors of histamine.
摘要翻译：使用式（A）化合物，其中：W是当连接到4（5）位的咪唑环时，其在组胺H3受体中具有拮抗作用和/或激动作用的残基; R 1和R 2可以相同或不同，各自独立地表示低级烷基或环烷基，或与它们所连接的氮原子一起，与所定义的饱和含氮环（i）一起形成非芳族不饱和氮 - （ii）定义的吗啉基或N-取代的哌嗪子基团，其用于制备组胺的H3受体作为拮抗剂和/或激动剂的药物。

6. 发明申请

US20110028562A1 DERIVATIVES OF AMINOALKANOLS, METHOD OF OBTAINING OF AMINOALKANOLS AND THEIR USE 有权
标题翻译：氨基烷醇的衍生物，获得氨基烷醇的方法及其用途
公开(公告)号：US20110028562A1
公开(公告)日：2011-02-03
申请号：US12863881
申请日：2009-01-19
申请人： Henryk Marona , Anna Waszkielewicz , Katarzyna Kiec-Kononowicz
发明人： Henryk Marona , Anna Waszkielewicz , Katarzyna Kiec-Kononowicz
IPC分类号： A61K31/165 , C07C215/08 , A61K31/138 , A61P25/12 , A61P29/00 , C07C233/18
CPC分类号： C07C217/18 , C07B2200/07 , C07C217/16 , C07C217/20 , C07C235/20 , C07C235/22 , C07C237/22 , C07C2601/14
摘要： The subject of the invention is a group of new derivatives of aminoalkaπols, more specifically [(phenoxy)alkyl]aminoalkanols and [(phenoxy)acyl)aminoalkanols, their method of obtaining and their use for production of a medicine which is used in the prophylaxis, prevention and/or treatment of diseases or symptoms having neurological background and for production of a medicine with anticonvulsant activity, which is used in seizures of various origin, also in the limbic system, in myoclonic or sound-induced seizures, in psychomotor epilepsy, as well as in relieving neuropathic or inflammatory pain.
摘要翻译：本发明的主题是一组氨基酸和更多的[（苯氧基）烷基]氨基链烷醇和[（苯氧基）酰基）氨基链烷醇的新衍生物，其获得方法及其用于生产药物的方法，其用于预防，预防和/或治疗具有神经系统背景的疾病或症状，并用于生产具有抗惊厥活性的药物，其用于各种起源的缉获，也用于边缘系统，肌阵挛或声音诱发性癫痫发作，精神运动癫痫，以及缓解神经性或炎性疼痛。

7. 发明申请

US20100029624A1 Male Contraceptive 有权
标题翻译：男性避孕药
公开(公告)号：US20100029624A1
公开(公告)日：2010-02-04
申请号：US12504287
申请日：2009-07-16
申请人： Nnaemeka Ikechukwu AMOBI , Ian Christopher SMITH
发明人： Nnaemeka Ikechukwu AMOBI , Ian Christopher SMITH
IPC分类号： A61K31/5415 , A61K31/473 , A61K31/472 , A61K31/47 , A61K31/445 , A61K31/4402 , A61K31/40 , A61K31/136 , A61P15/00
CPC分类号： C07C211/27 , C07C211/45 , C07C217/16 , C07C2603/26 , C07D207/09 , C07D209/08 , C07D211/12 , C07D211/14 , C07D211/26 , C07D215/06 , C07D215/12 , C07D217/10 , C07D221/04 , C07D279/26 , C07D279/28 , C07D295/03 , C07D401/06 , C07D417/06
摘要： A compound having formula I. R1, R2, R3 and R4 are independently H or lower alkyl. R5 is aryl, heteroaryl, cycloalkyl, heterocycloalkyl, aryloxy, heteroaryloxy, cycloalkyloxy, heterocycloalkyloxy, arylamino, heteroarylamino, cycloalkylamino, heterocycloalkyl amino, arylthio, heteroarylthio, cycloalkylthio, heterocycloalkylthio, or cyclic olefin, any of which may be substituted or non-substituted; or substituted alkyl, substituted alkyl oxy or substituted alkyl amino wherein the substituent is an aryl, a heteroaryl, a cycloalkyl, a heterocycloalkyl or a cyclic olefin, any of which may be substituted or non-substituted. X is C or N. n and p are independently whole numbers selected from 0, 1 and 2. (CH2)n and (CH2)p may be substituted or non-substituted. Ar1 and Ar2 are independently aryl or heteroaryl groups which may be substituted or non-substituted. Certain specific compounds are excluded.The compounds can be used in a medicament or a method for the reduction or prevention of the emission of sperm, or for the reduction or prevention of transmission of viral agents transmitted in seminal fluid.
摘要翻译：具有式I的化合物.R 1，R 2，R 3和R 4独立地为H或低级烷基。 R5是芳基，杂芳基，环烷基，杂环烷基，芳氧基，杂芳氧基，环烷氧基，杂环烷氧基，芳基氨基，杂芳基氨基，环烷基氨基，杂环烷基氨基，芳硫基，杂芳硫基，环烷硫基，杂环烷硫基或环烯烃，其中任何一个可以是取代或未取代的; 或取代的烷基，取代的烷基氧基或取代的烷基氨基，其中取代基是芳基，杂芳基，环烷基，杂环烷基或环烯烃，其中任何一个可以被取代或未取代。 X是C或N.n，p独立地是选自0,1和2的整数。（CH 2）n和（CH 2）p可以是取代或未取代的。 Ar 1和Ar 2独立地为可被取代或未取代的芳基或杂芳基。排除某些具体化合物。这些化合物可以用于减少或预防精子发射的药物或方法，或用于减少或防止在精液中传播的病毒剂的传播。

8. 发明授权

US07569729B2 Stable atomoxetine hydrochloride, a process for the preparation thereof, and an analytical control of its stability 失效
标题翻译：稳定的阿托西汀盐酸盐，其制备方法及其稳定性的分析控制
公开(公告)号：US07569729B2
公开(公告)日：2009-08-04
申请号：US11399055
申请日：2006-04-05
申请人： Eugenio Castelli , Paolo Riva
发明人： Eugenio Castelli , Paolo Riva
IPC分类号： C07C213/10 , C07C211/27 , A61K31/135
CPC分类号： C07C217/16 , C07C213/10 , C07C217/48
摘要： Stable Atomoxetine hydrochloride, a process for the manufacture thereof, the use of stable Atomoxetine Hydrochloride for making a pharmaceutical formulation, a process for the preparation of any form of Atomoxetine Hydrochloride, and an analytical method for analyzing the stability of Atomoxetine Hydrochloride are provided.
摘要翻译：稳定的阿莫西汀盐酸盐，其制备方法，使用稳定的盐酸阿托西汀制备药物制剂，制备任何形式的阿托莫西汀盐酸盐的方法，以及分析盐酸阿托西汀的稳定性的分析方法。

9. 发明申请

US20080207725A1 Phenyl-Pyrazole Derivatives as Non-Steroidal Glucocorticoid Receptor Ligands 审中-公开
标题翻译：苯基吡唑衍生物作为非甾体糖皮质激素受体配体
公开(公告)号：US20080207725A1
公开(公告)日：2008-08-28
申请号：US11917775
申请日：2006-06-27
申请人： Michael David Barker , David House , Haydn Terence Jones , Simon John Fawcett MacDonald , Iain McFarlane Mclay
发明人： Michael David Barker , David House , Haydn Terence Jones , Simon John Fawcett MacDonald , Iain McFarlane Mclay
IPC分类号： A61K31/415 , C07D403/12 , C07D231/38 , A61P29/00 , A61P37/00 , A61P17/00 , A61K9/12 , A61K31/4155
CPC分类号： C07C215/28 , C07B2200/07 , C07C217/16 , C07D231/38 , C07D307/79 , C07D405/12
摘要： A compound of formula (I): wherein A represents 2,3-dihydro-1-benzofuran-7-yl, 5-fluoro-2-methoxy-phenyl or 5-fluoro-2-hydroxy-phenyl; and R1 and R2 each independently represent hydrogen, fluorine or chlorine; or a physiologically functional derivative thereof.
摘要翻译：式（I）的化合物：其中A表示2,3-二氢-1-苯并呋喃-7-基，5-氟-2-甲氧基 - 苯基或5-氟-2-羟基 - 苯基; R 1和R 2各自独立地表示氢，氟或氯; 或其生理功能衍生物。

10. 发明申请

US20060252836A1 Stable atomoxetine hydrochloride, a process for the preparation thereof, and an analytical control of its stability 失效
公开(公告)号：US20060252836A1
公开(公告)日：2006-11-09
申请号：US11399055
申请日：2006-04-05
申请人： Eugenio Castelli , Paolo Riva
发明人： Eugenio Castelli , Paolo Riva
IPC分类号： A61K31/138 , C07C215/34
CPC分类号： C07C217/16 , C07C213/10 , C07C217/48
摘要： Stable Atomoxetine hydrochloride, a process for the manufacture thereof, the use of stable Atomoxetine Hydrochloride for making a pharmaceutical formulation, a process for the preparation of any form of Atomoxetine Hydrochloride, and an analytical method for analyzing the stability of Atomoxetine Hydrochloride are provided.

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