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81. 发明申请

US20090131402A1 Fused heterocyclic compound and use thereof 有权
标题翻译：稠合杂环化合物及其用途
公开(公告)号：US20090131402A1
公开(公告)日：2009-05-21
申请号：US12227333
申请日：2007-05-15
申请人： Junya Shirai , Tomokazu Kusumoto , Hiroyuki Nagamiya , Izumi Kamo
发明人： Junya Shirai , Tomokazu Kusumoto , Hiroyuki Nagamiya , Izumi Kamo
IPC分类号： A61K31/553 , C07D498/04 , A61P3/04 , A61K31/4353 , A61B5/103
CPC分类号： A61K31/553 , A61B5/04882 , A61B5/202 , A61B5/205 , A61K31/00 , A61K31/4353 , A61N1/36007 , C07D223/16 , C07D487/04 , C07D498/04 , C07D519/00 , G01N33/942
摘要： The present invention relates to a serotonin 5-HT2C receptor activator containing a compound represented by the formula wherein ring A is a 5- or 6-membered aromatic heterocycle optionally having substituent(s), and ring B is a 7- to 9-membered ring optionally having substituent(s) other than an oxo group wherein the combination of m and n (m,n) is (1,2), (2,1), (2,2), (3,1), (3,2) or (4,1), or a salt thereof or a prodrug thereof, and a fused heterocyclic compound having a serotonin 5-HT2C receptor activating action and the like.
摘要翻译：本发明涉及含有下式表示的化合物的5-羟色胺5-HT 2C受体活化剂，其中环A是任选具有取代基的5-或6-元芳族杂环，环B为7-至9-元其中m和n（m，n）的组合是（1,2），（2,1），（2,2），（3,1），（ 3,2）或（4,1）或其盐或其前药，以及具有5-羟色胺5-HT 2C受体激活作用的稠合杂环化合物等。

82. 发明申请

US20090110713A1 Biodegradable polymeric materials providing controlled release of hydrophobic drugs from implantable devices 审中-公开
标题翻译：提供可植入式设备的疏水性药物的控制释放的可生物降解的聚合材料
公开(公告)号：US20090110713A1
公开(公告)日：2009-04-30
申请号：US11982160
申请日：2007-10-31
申请人： Florencia Lim , Michael H. Ngo , Yiwen Tang , Syed F.A. Hossainy , Mikael O. Trollsas
发明人： Florencia Lim , Michael H. Ngo , Yiwen Tang , Syed F.A. Hossainy , Mikael O. Trollsas
IPC分类号： A61F2/82 , C08L5/00 , C08L5/06 , C08L3/00 , C08L1/00 , C08G63/00 , C08G63/08 , A61K47/30 , A61K31/4353
CPC分类号： C08G63/08 , A61L31/06 , A61L31/10 , A61L31/16 , A61L2300/602 , C08L67/04
摘要： The present invention is directed to polymeric materials (e.g., coatings) comprising biodegradable copolymers and implantable devices (e.g., drug-delivery stents) formed of such materials. The biodegradable copolymers are derived from at least two relatively polar monomers and at least one relatively nonpolar monomer. Incorporation of at least one relatively nonpolar monomer into the copolymer improves controlled release of a hydrophobic drug from the polymeric material by increasing the copolymer's miscibility with and permeability to the hydrophobic drug. The polymeric materials can also contain at least one biocompatible moiety, at least one non-fouling moiety, at least one biobeneficial material, at least one bioactive agent, or a combination thereof. The polymeric materials are designed to improve the mechanical, physical and biological properties of implantable devices formed thereof.
摘要翻译：本发明涉及包含由这种材料形成的可生物降解的共聚物和可植入装置（例如药物递送支架）的聚合物材料（例如包衣）。可生物降解的共聚物衍生自至少两种相对极性的单体和至少一种相对非极性的单体。将至少一种相对非极性的单体掺入共聚物中，通过增加共聚物与疏水性药物的混溶性和渗透性，可以改善疏水性药物从聚合物材料的受控释放。聚合物材料还可含有至少一种生物相容部分，至少一种非结垢部分，至少一种生物有益材料，至少一种生物活性剂或其组合。聚合材料被设计成改善由其形成的可植入装置的机械，物理和生物学特性。

83. 发明申请

US20080317853A1 Mouth Dissolving Pharmaceutical Composition and Process for Preparing the Same 有权
标题翻译：口溶解药物组合物及其制备方法
公开(公告)号：US20080317853A1
公开(公告)日：2008-12-25
申请号：US12097813
申请日：2006-08-30
申请人： Namdev Kashid , Gour Mukherji
发明人： Namdev Kashid , Gour Mukherji
IPC分类号： A61K9/20 , A61K31/167 , A61K31/551 , A61K31/4353 , A61K31/546 , A61K31/4545
CPC分类号： A61K9/0056 , A61K9/0007 , A61K9/2018 , A61K9/2077 , A61K9/2095 , A61K31/167 , A61K31/445 , A61K31/54 , A61K31/551 , A61K31/5513
摘要： Disclosed herein is a orally disintegrating and/or dissolving oral pharmaceutical composition, comprising one or more active pharmaceutical ingredients, one or more fillers having particle size of 100 microns or above, a high and desirable amount of silicon dioxide, one or more disintegrating agents, optionally effervescent couple, wherein said composition has good organoleptic properties like desired mouth feel and fast oral disintegration time.
摘要翻译：本文公开了口腔崩解和/或溶解的口服药物组合物，其包含一种或多种活性药物成分，一种或多种粒度为100微米或更高的填料，高和所需量的二氧化硅，一种或多种崩解剂，任选的泡腾对，其中所述组合物具有良好的感官特性，如期望的口感和快速的口服崩解时间。

84. 发明申请

US20080311223A1 INJECTABLE POLYMER-LIPID BLEND FOR LOCALIZED DRUG DELIVERY 审中-公开
标题翻译：用于局部药物输送的可注射聚合物 - 脂质混合物
公开(公告)号：US20080311223A1
公开(公告)日：2008-12-18
申请号：US12138141
申请日：2008-06-12
申请人： Christine ALLEN , Justin Grant , Jaepyoung Cho , Patrick Lim Soo , Micheline Piquette-Miller
发明人： Christine ALLEN , Justin Grant , Jaepyoung Cho , Patrick Lim Soo , Micheline Piquette-Miller
IPC分类号： A61K33/24 , A61K47/36 , A61K31/17 , A61K31/505 , A61K31/66 , A61K31/397 , A61K31/4353 , A61K38/02 , A61K31/7052 , A61P35/00 , A61K38/16 , A61K31/704 , A61K31/403 , A61K31/4164 , A61K38/10 , A61K31/4985 , A61K31/282
CPC分类号： A61K31/337 , A61K9/0024 , A61K47/08 , A61K47/12 , A61K47/24 , A61K47/36
摘要： An injectable polymer-lipid blend is provided as a localized drug delivery system for a pharmaceutically active agent. The blend may be prepared from a chitosan-based material, fatty acid and phospholipid. The chitosan-based material may be a water soluble chitosan derivative. The fatty acid may be a fatty acid or a fatty aldehyde, such as laurinaldehyde, having an acyl chain length of C8-C16. The rheological properties of the blend relates to the ratio of the components and to the acyl chain length of the fatty acid. The injectable system is well suited for the delayed release of pharmaceutically active agents in the treatment of cancer and other diseases requiring localized drug delivery.
摘要翻译：提供可注射的聚合物 - 脂质混合物作为药物活性剂的局部药物递送系统。共混物可以由壳聚糖基材料，脂肪酸和磷脂制备。基于壳聚糖的材料可以是水溶性壳聚糖衍生物。脂肪酸可以是酰基链长度为C8-C16的脂肪酸或脂肪醛，例如月桂醛。共混物的流变特性涉及组分与脂肪酸的酰基链长度的比例。注射系统非常适合药物活性剂在治疗癌症和需要局部药物递送的其它疾病中的延迟释放。

85. 发明申请

US20080262014A1 Use of Camptothecin Derivatives for the Treatment of Proliferative Diseases in a Fixed Dosing Regimen 审中-公开
标题翻译：喜树碱衍生物在固定剂量方案中用于增殖性疾病的治疗
公开(公告)号：US20080262014A1
公开(公告)日：2008-10-23
申请号：US10592832
申请日：2005-03-24
申请人： Horst F. Schran , Margaret Ma Woo
发明人： Horst F. Schran , Margaret Ma Woo
IPC分类号： A61K31/4353 , A61P35/00
CPC分类号： A61K31/4745
摘要： Topoisomerase I inhibitors are administered for the treatment of proliferative diseases according to a once every three day fixed dosing regimens. Furthermore, the invention provides the use of topoisomerase inhibitors to manufacture a medicament which can be used in a fixed dose treatment regimen.
摘要翻译：根据每3天固定给药方案一次，施用拓扑异构酶I抑制剂用于治疗增殖性疾病。此外，本发明提供拓扑异构酶抑制剂用于制造可以以固定剂量治疗方案使用的药物的用途。

86. 发明申请

US20080260845A1 MULTIPLE ACTIVE DRUG RESIN CONJUGATE 审中-公开
标题翻译：多种活性药物结合剂
公开(公告)号：US20080260845A1
公开(公告)日：2008-10-23
申请号：US12059266
申请日：2008-03-31
申请人： Deepak Thassu , Paul D. Hafey , Sreekant R. Nadkarni , Jatin S. Desai , Leo J. Magee
发明人： Deepak Thassu , Paul D. Hafey , Sreekant R. Nadkarni , Jatin S. Desai , Leo J. Magee
IPC分类号： A61K9/14 , A61K31/4353 , A61K31/4439 , A61P43/00
CPC分类号： A61K31/485 , A61K31/4402 , A61K31/46 , A61K45/06 , A61K47/585 , A61K2300/00
摘要： A combination pharmaceutical preparation including two different active drugs of the same ionic charge conjugated with a single resin particle, without one significantly displacing the other, and without retarding the initial availability of either active. Also, methods for the manufacture of a multiple active drug-resin conjugate, and for the in vivo release of a combination of pharmaceutically active drugs from a multiple active drug-resin conjugate.
摘要翻译：包含与单个树脂颗粒缀合的相同离子电荷的两种不同活性药物的组合药物制剂，没有显着移位另一种，并且不会延迟任一活性物质的初始可用性。此外，制备多活性药物 - 树脂缀合物的方法以及用于从多活性药物 - 树脂缀合物体内释放药物活性药物的组合的方法。

87. 发明申请

US20080254029A1 Use of an Inhibitor of TNFa Plus an Antihistamine to Treat Allergic Rhinitis and Allergic Conjunctivitis 审中-公开
标题翻译：使用抑制TNFa Plus抗组胺药治疗过敏性鼻炎和过敏性结膜炎
公开(公告)号：US20080254029A1
公开(公告)日：2008-10-16
申请号：US12100715
申请日：2008-04-10
申请人： John M. Yanni , Daniel A. Gamache , Steven T. Miller , Clay Beauregard
发明人： John M. Yanni , Daniel A. Gamache , Steven T. Miller , Clay Beauregard
IPC分类号： A61K39/395 , A61K31/551 , A61K31/335 , A61K31/55 , A61P37/08 , A61K38/16 , A61K31/4353 , A61K31/52
CPC分类号： A61K45/06 , A61K31/335 , A61K31/551 , A61K38/191 , A61K39/395 , A61K2300/00
摘要： Disclosed are methods of treating allergic conjunctivitis and allergic rhinitis in a subject that involve topically administering to the subject a composition comprising a pharmaceutically effective amount of an H1 antagonist and an anti-TNFα compound.
摘要翻译：公开了治疗过敏性结膜炎和过敏性鼻炎的方法，其涉及向受试者局部施用包含药学有效量的H 1拮抗剂和抗TNFα化合物的组合物。

88. 发明申请

US20080242649A1 New Combination 665 审中-公开
标题翻译：新组合665
公开(公告)号：US20080242649A1
公开(公告)日：2008-10-02
申请号：US12027424
申请日：2008-02-07
申请人： Elaine Bridget Cadogan , Stephen Connolly , David John Nicholls , Katherine Elisabeth Wiley , Alan Young
发明人： Elaine Bridget Cadogan , Stephen Connolly , David John Nicholls , Katherine Elisabeth Wiley , Alan Young
IPC分类号： A61K31/428 , A61K31/4353 , A61K31/56 , A61P11/06 , A61P11/00
CPC分类号： A61K45/06 , A61K31/428 , A61K2300/00
摘要： The invention provides a pharmaceutical product comprising a first active ingredient which is N—[2-(Diethylamino)ethyl]-N-(2-{[2-(4-hydroxy-2-oxo-2,3-dihydro-1,3-benzothiazol-7-yl)ethyl]amino}ethyl)-3-[2-(1-naphthyl)ethoxy]propanamide or a salt thereof, and a second active ingredient selected from: a non-steroidal Glucocorticoid Receptor (GR Receptor) Agonist; an antioxidant; a CCR1 antagonist; a chemokine antagonist (not CCR1); a corticosteroid; a CRTh2 antagonist; a DP1 antagonist; an Histone Deacetylase Inducer; an IKK2 inhibitor; a COX inhibitor; a lipoxygenase inhibitor; a leukotriene receptor antagonist; an MPO inhibitor; a muscarinic antagonist which is Aclidinium bromide, Glycopyrrolate, Oxitropium bromide, Pirenzepine, telenzepine, Tiotropium bromide, 3(R)—(2-hydroxy-2,2-dithien-2-ylacetoxy)-1-(3-phenoxypropyl)-1-azoniabicyclo[2.2.2]octane bromide, 3(R)—1-phenethyl-3-(9H-xanthene-9-carbonyloxy)-1-azoniabicyclo[2.2.2]octane bromide or (3R)—3-[(2S)—2-cyclopentyl-2-hydroxy-2-thien-2-ylacetoxy]-1-(2-phenoxyethyl)-1-azoniabicyclo[2.2.2]actane bromide; a p38 inhibitor; a PDE inhibitor; a PPARγ agonist; a protease inhibitor; a Statin; a thromboxane antagonist; a vasodilator; or, an ENAC blocker (Epithelial Sodium-channel blocker); and its use in the treatment of respiratory disease.
摘要翻译：本发明提供包含第一活性成分的药物产品，其为N- [2-（二乙基氨基）乙基] -N-（2 - {[2-（4-羟基-2-氧代-2,3-二氢-1,2- 3-苯并噻唑-7-基）乙基]氨基}乙基）-3- [2-（1-萘基）乙氧基]丙酰胺或其盐，和第二活性成分，选自：非甾体糖皮质激素受体（GR受体）激进者抗氧化剂 CCR1拮抗剂; 趋化因子拮抗剂（不是CCR1）; 皮质类固醇 CRTh2拮抗剂; DP1拮抗剂; 组蛋白脱乙酰酶诱导剂; IKK2抑制剂; COX抑制剂; 脂氧合酶抑制剂; 白细胞三烯受体拮抗剂; MPO抑制剂; 吖啶啶溴化物，乙酰丙酸乙酯，溴化氧氮，哌仑西平，替硝西泮，噻托溴铵，3（R） - （2-羟基-2,2-二噻吩-2-基乙酰氧基）-1-（3-苯氧基丙基）-1 （R）-1-苯乙基-3-（9H-呫吨-9-羰氧基）-1-氮鎓二环[2.2.2]辛烷溴化物或（3R）-3 - [（ 2S）-2-环戊基-2-羟基-2-噻吩-2-基乙酰氧基] -1-（2-苯氧基乙基）-1-氮鎓二环[2.2.2] 一种p38抑制剂; PDE抑制剂; 一种PPARγ激动剂; 蛋白酶抑制剂; 他汀类血栓素拮抗剂; 血管扩张剂或ENAC阻断剂（上皮钠通道阻断剂）; 并用于治疗呼吸系统疾病。

89. 发明申请

US20080175932A1 Method for Decreasing Nicotine and Other Substance Use in Humans 审中-公开
公开(公告)号：US20080175932A1
公开(公告)日：2008-07-24
申请号：US12013089
申请日：2008-01-11
申请人： Jie Wu
发明人： Jie Wu
IPC分类号： A61K36/18 , A61K31/4353 , A61P25/34 , A61P25/30 , A61P25/00
CPC分类号： A61K36/185
摘要： A method for decreasing nicotine and other substance use in humans is disclosed. Tetrahydroberberine (THB) and its analogs, l-Tetrahydropalmatine (l-THP) and l-Stepholidine (l-SPD), are present in and can be isolated from several plants in the Magnoliidae superorder. According to the disclosed method, THB and its analogs are used to block nicotine-induced DA release, and modulate heterologous or homoeric expression of human nicotinic acetylcholine receptors (nAChR) in humans. Specifically, THB exhibits bi-directory modulation of α4β2-nAChR-mediated currents induced by nicotine. THB also shows predominant inhibition on homologously expressed α7-nAChR function. Thus, according to the disclosed method, THB is used to simultaneous blockade midbrain DA system function, the brain reward center, and neuronal α4β2- and α7-nAChR function, the major nicotine targets in the brain. Therefore, THB and its analogs serve as a novel class of natural compounds to decrease nicotine dependence in humans. Furthermore other substances, such as alcohol, cocaine, and opiates, also operate by triggering the brain reward center, resulting in a cycle of substance or alcohol abuse. THB and its analogs can be used to decrease use of substances such as alcohol, cocaine, and opiates. Finally, because THB and its analogs are DA antagonists, THB and its analogs can also be used as a treatment for Parkinson's Disease, Alzheimer's Disease and Schizophrenia.

90. 发明授权

US07399769B2 Aryl-isoxazol-4-yl-imidazo[1,5-a]pyridine derivatives 失效
标题翻译：芳基异恶唑-4-基 - 咪唑并[1,5-a]吡啶衍生物
公开(公告)号：US07399769B2
公开(公告)日：2008-07-15
申请号：US11640768
申请日：2006-12-18
申请人： Bernd Buettelmann , Jiaqiang Dong , Bo Han , Henner Knust , Andrew Thomas
发明人： Bernd Buettelmann , Jiaqiang Dong , Bo Han , Henner Knust , Andrew Thomas
IPC分类号： A61K31/4353 , C07D471/02
CPC分类号： C07D471/04
摘要： The present invention is concerned with aryl-isoxazol-4-yl-imidazo[1,5-a]pyridine derivatives of formula wherein: R1, R2, and R3 are as defined herein and pharmaceutically acceptable acid addition salts thereof. These compounds have high affinity and selectivity for GABA A α5 receptor binding sites. The invention also relates to methods for enhancing cognition and treating cognitive disorders like Alzheimer's disease.
摘要翻译：本发明涉及下式的芳基 - 异恶唑-4-基 - 咪唑并[1,5-a]吡啶衍生物其中：R 1，R 2，R 2，R 3和本文所定义的药学上可接受的酸加成盐。这些化合物对GABA Aα5受体结合位点具有高亲和力和选择性。本发明还涉及用于增强认知和治疗认知障碍如阿尔茨海默病的方法。

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