公开(公告)号：US20040024001A1

公开(公告)日：2004-02-05

申请号：US10423788

申请日：2003-04-25

发明人： William J. Pitts ,  Soong-Hoon Kim ,  Joseph Barbosa ,  Wayne Vaccaro

IPC分类号： A61K031/515 ,  C07D487/10

CPC分类号： C07D487/10

摘要： Compound having the formula (I), 1 wherein A, B and D are O or S; R1a and R1b are H, C1-4alkyl, C2-4alkenyl, or C2-4alkynyl; X is nullNR2null, nullSnull, nullS(nullO)null, or nullS(O)2null; G1, G2 and G3 are together or separately selected from hetero, carbonyl, alkylene, and alkenylene groups and G4 is optionally substituted methylene; R2 is Q-Ar, wherein Q is a linker and Ar is substituted or substituted aryl or heteroaryl; and z is 0 or 1, are useful as inhibitors of MMPs, particularly MMP-13, aggrecanase, and/or TACE.

摘要翻译： 具有式（I）的化合物，其中A，B和D为O或S; R1a和R1b是H，C1-4烷基，C2-4链烯基或C2-4炔基; X是-NR 2 - ， - S - ， - S（= O） - 或-S（O）2 - ; G1，G2和G3一起或分别选自杂，羰基，亚烷基和亚烯基，G4是任选取代的亚甲基; R2是Q-Ar，其中Q是连接基，Ar是取代或取代的芳基或杂芳基; 和z为0或1，可用作MMP的抑制剂，特别是MMP-13，聚集蛋白聚糖蛋白聚糖酶和/或TACE。

公开(公告)号：US20030232849A1

公开(公告)日：2003-12-18

申请号：US10424382

申请日：2003-04-28

申请人： Pfizer Inc.

发明人： Mark C. Noe ,  Lilli Ann Wolf-Gouveia

IPC分类号： A61K031/515 ,  C07D43/02

CPC分类号： C07D401/14 ,  C07D403/12 ,  C07D403/14

摘要： The present invention relates to N-substituted-heteroaryloxy-aryloxy-2,4,6-trione metalloproteinase inhibitors of the formula 1 wherein X, A, Y, B, G, and R1 are as defined in the specification, and to pharmaceutical compositions and methods of treating inflammation, cancer and other disorders.

摘要翻译： 本发明涉及下式的N-取代 - 杂芳氧基 - 芳氧基-2,4,6-三酮金属蛋白酶抑制剂，其中X，A，Y，B，G和R 1如说明书中所定义， 治疗炎症，癌症和其他疾病的药物组合物和方法。

公开(公告)号：US20030187005A1

公开(公告)日：2003-10-02

申请号：US10354146

申请日：2003-01-30

申请人： Taro Pharmaceutical Industries Ltd.

发明人： Daniella Gutman ,  Daniel A. Moros

IPC分类号： A61K031/515

CPC分类号： A61K31/675 ,  A61K31/515

摘要： The present invention relates to novel non-sedating barbituric acid derivatives, pharmaceutical compositions containing them and methods of neuroprotection in cases of cerebral ischemia, head trauma and other acute neurologic injuries, and prevention of resulting neuronal damage. The invention also relates to the use of non-sedating barbituric acid derivatives given in a manner and dosage effective to produce blood levels and brain levels of these drugs and/or their active metabolites sufficient to provide a therapeutic effect.

摘要翻译： 本发明涉及新型非镇静巴比妥酸衍生物，含有它们的药物组合物和脑缺血，头部创伤和其他急性神经损伤情况下神经保护的方法，以及预防所产生的神经元损伤。 本发明还涉及以有效的方式和剂量给出的非镇静性巴比妥酸衍生物用于产生足以提供治疗效果的这些药物和/或其活性代谢物的血液水平和脑水平的用途。

公开(公告)号：US20030027833A1

公开(公告)日：2003-02-06

申请号：US10141496

申请日：2002-05-07

发明人： Gary W. Cleary ,  Sri Mudumba ,  Shohreh Parandoosh ,  Colin J. Cleary ,  Raj Birudaraj ,  Pathamar Park

IPC分类号： A61K031/515 ,  A61K031/24 ,  A61K031/02 ,  A61K031/46

CPC分类号： A61K9/0014 ,  A61K9/7015 ,  A61K31/165 ,  A61K31/245 ,  A61K47/10 ,  A61K47/14 ,  A61K47/32 ,  A61K47/36 ,  A61K47/40

摘要： A pharmaceutical composition is provided for topical administration of a local anesthetic agent. The composition comprises (a) a therapeutically effective amount of a local anesthetic agent and (b) a pharmaceutically acceptable, nonliposomal carrier comprised of a monohydric alcohol, a penetration enhancer, and polymer, which may be a hydrophilic polymer, a hydrophobic polymer or a combination thereof. The composition can be in the form of a gel, or it may form a film following application to a patient's body surface and evaporation of the monohydric alcohol. The composition provides rapid onset of local anesthesia as well as penetration of the active agent into the skin. Methods and drug delivery systems for administration of local anesthetic agents are also provided.

摘要翻译： 提供用于局部施用局部麻醉剂的药物组合物。 组合物包含（a）治疗有效量的局部麻醉剂和（b）由一元醇，渗透增强剂和聚合物组成的药学上可接受的非脂质载体，其可以是亲水性聚合物，疏水性聚合物或 的组合。 组合物可以是凝胶的形式，或者可以在施用于患者的身体表面并蒸发一元醇后形成膜。 该组合物可快速开始局部麻醉以及活性剂渗入皮肤。 还提供了用于施用局部麻醉剂的方法和药物递送系统。

公开(公告)号：US20020165246A1

公开(公告)日：2002-11-07

申请号：US10091744

申请日：2002-03-05

发明人： Andrew Holman

IPC分类号： A61K031/515

CPC分类号： A61K31/47 ,  A61K31/545 ,  A61K31/675 ,  A61K2300/00

摘要： The present invention provides methods and compositions for increasing the efficacy of a therapeutic agent administered to a subject. A sleep restorative agent is co-administered to the subject along with the therapeutic agent, whereby the efficacy of the therapeutic agent is increased.

摘要翻译： 本发明提供了用于增加施用于受试者的治疗剂的功效的方法和组合物。 睡眠修复剂与治疗剂一起共同施用于受试者，由此增加治疗剂的功效。

公开(公告)号：US20040224006A1

公开(公告)日：2004-11-11

申请号：US10829143

申请日：2004-04-21

发明人： Samn Raffaniello

IPC分类号： A61K038/48 ,  A61K031/515 ,  A61K031/19

CPC分类号： A61K38/482 ,  A61K31/00 ,  A61K31/19 ,  A61K31/515 ,  A61K38/166 ,  A61K38/49 ,  A61L15/44 ,  A61L17/005 ,  A61L2300/254 ,  A61L2300/30 ,  A61L2300/42

摘要： A method for minimizing scarring and preventing excessive scar formation at an injury site is disclosed. The method involves the topical and/or local application of a therapeutically effective amount of a defibrinogenating agent or of a fibrinolytic agent that may be delivered in an appropriate vehicle in a controlled- or timed-release manner. In accordance with the principles of the invention, the defibrinogenating agent or fibrinolytic agent is applied as a coating on, or is irradiated or impregnated into or onto a delivery vehicle such as, for example, sutures, dissolvable sutures, bandages, gauze pads, or other types of first aid bandaging materials. Such application may take the form of a controlled- or timed-release aspect of either the vehicle, the delivery material or the therapeutic agent, such that the release of the therapeutic agent may be regulated to produce an appropriate therapeutic pattern or defibrinogenation or fibrinolysis. In a preferred aspect of the invention, the defibrinogenating agent is ancrod, and the mode of application is as ancrod-coated sutures.

摘要翻译： 公开了一种减少瘢痕形成并防止损伤部位过度瘢痕形成的方法。 该方法涉及局部和/或局部施用治疗有效量的去纤维蛋白原化剂或纤维蛋白溶解剂，其可以以受控或定时释放的方式递送于合适的载体中。 根据本发明的原理，脱纤维蛋白原化剂或纤维蛋白溶解剂作为涂层施用于或被照射或浸渍到递送载体中或载体上，例如缝合线，可溶解缝线，绷带，纱布垫或 其他类型的急救包扎材料。 这种应用可以采取车辆，递送材料或治疗剂的受控制或定时释放方面的形式，使得可以调节治疗剂的释放以产生适当的治疗模式或去纤维蛋白原化或纤维蛋白溶解。 在本发明的优选方面，除纤维蛋白原化剂是辅助的，并且应用的方式是作为辅助涂层的缝合线。

公开(公告)号：US20040214845A1

公开(公告)日：2004-10-28

申请号：US10848718

申请日：2004-05-19

申请人： Millennium Pharmaceuticals, Inc.

发明人： Marc Bazin ,  Geraldine C. Harriman ,  Cyrille Kuhn ,  Jay R. Luly

IPC分类号： A61K031/515

CPC分类号： C07D401/06 ,  A61K31/515 ,  C07D239/62 ,  C07D401/14 ,  C07D403/04 ,  C07D403/06 ,  C07D403/14 ,  C07D405/04 ,  C07D405/06 ,  C07D405/14 ,  C07D409/06

摘要： The invention relates to a pharmaceutical composition comprising a compound of the formula (I): 1 in which X is O or S; R1 is hydrogen or null(CH2)nnullAr1; R2 is hydrogen or has the same meaning as R1; R3 is Ar2 or null(CHnullCH)nullAr2 where Ar2 has the same meaning as Ar1; together with a pharmaceutically acceptable carrier. The invention also relates to a method of treating an individual suffering from a disease associated with leukocyte infiltration of tissues expressing the molecule MAdCAM-1, comprising administering a therapeutically effective amount of a compound of formula (I). The invention also relates to a method of inhibiting the binding of a cell expressing a ligand for MAdCAM-1 on its surface to MAdCAM-1 or a portion thereof. The invention further relates to a method of preparing a pharmaceutical composition comprising a compound of the formula (I).

摘要翻译： 本发明涉及包含式（I）化合物的药物组合物：其中X为O或S; R1是氢或 - （CH2）n-Ar1; R2是氢或具有与R1相同的含义; R3是Ar2或 - （CH = CH）-Ar2，其中Ar2与Ar1具有相同的含义; 以及药学上可接受的载体。 本发明还涉及治疗患有与表达分子MAdCAM-1的组织的白细胞浸润相关的疾病的个体的方法，其包括施用治疗有效量的式（I）化合物。 本发明还涉及抑制表达MAdCAM-1配体的细胞与MAdCAM-1或其部分结合的方法。 本发明还涉及制备包含式（I）化合物的药物组合物的方法。

公开(公告)号：US20040106600A1

公开(公告)日：2004-06-03

申请号：US10601070

申请日：2003-06-20

发明人： Carl-Magnus Andersson ,  Nathalie Schlienger ,  Alma Fejzic ,  Eva Louise Hansen ,  Jan Pawlas

IPC分类号： A61K031/55 ,  A61K031/541 ,  A61K031/5377 ,  A61K031/535 ,  A61K031/515 ,  A61K031/496 ,  A61K031/453 ,  A61K031/452

CPC分类号： C07D401/06 ,  C07D405/06 ,  C07D405/14 ,  C07D413/06

摘要： Disclosed herein are compounds of Formula I, 1 or a pharmaceutically acceptable salt, amide, ester, or prodrug thereof. Also disclosed are. methods of inhibiting an activity of a monoamine receptor comprising contacting the monoamine receptor or a system containing the monoamine receptor with an effective amount of one or more of the compounds of Formula I. Disclosed are also methods of inhibiting an activation of a monoamine receptor comprising contacting the monoamine receptor or a system containing the monoamine receptor with an effective amount of one or more of the compounds of Formula I. Furthermore, methods of treating psychotic disease using a compound of Formula I are disclosed.

摘要翻译： 本文公开了式I的化合物或其药学上可接受的盐，酰胺，酯或前药。 还公开了。 抑制单胺受体活性的方法包括使单胺受体或含有单胺受体的系统与有效量的一种或多种式I化合物接触。还公开了抑制单胺受体活化的方法，包括接触 单胺受体或含有有效量的一种或多种式I化合物的单胺受体的体系。此外，公开了使用式I化合物治疗精神病的方法。

公开(公告)号：US20040062716A1

公开(公告)日：2004-04-01

申请号：US10663817

申请日：2003-09-17

申请人： NovaDel Pharma Inc.

发明人： Harry A. Dugger III

IPC分类号： A61K038/00 ,  A61L009/04 ,  A61K031/522 ,  A61K031/515 ,  A61K031/557

CPC分类号： A61K9/006 ,  A61K9/0056 ,  A61K9/124 ,  A61K31/085 ,  A61K31/137 ,  A61K31/138 ,  A61K31/197 ,  A61K31/27 ,  A61K31/4178 ,  A61K31/421 ,  A61K31/433 ,  A61K31/7076 ,  A61K38/13 ,  A61K47/06 ,  A61K47/14 ,  A61K47/44

摘要： Buccal aerosol sprays or capsule using polar and non-polar solvent have now been developed which provide biologically active compounds for rapid absorption through the oral mucosa, resulting in fast onset of effect. The buccal polar compositions of the invention comprises formulation I: polar solvent 37-98.58%, active compound 0.005-55%, optionally containing flavoring agent 0.1-10%.

摘要翻译： 现在已经开发了使用极性和非极性溶剂的颊气溶胶喷雾剂或胶囊，其提供用于通过口腔粘膜快速吸收的生物活性化合物，导致快速起效。 本发明的口腔极性组合物包含制剂I：极性溶剂37-98.58％，活性化合物0.005-55％，任选地含有调味剂0.1-10％。

公开(公告)号：US20020013330A1

公开(公告)日：2002-01-31

申请号：US09841738

申请日：2001-04-24

发明人： Pascal Druzgala ,  Peter G. Milner

IPC分类号： A61K031/515 ,  C07D43/02 ,  C07D239/08

CPC分类号： C07D239/62 ,  C07D239/66

摘要： The subject invention concerns novel compounds that are useful as ultrashort acting hypnotic barbiturates. Specifically exemplified are derivatives of barbituric and thiobarbituric acids. They are rapidly metabolized by blood and tissue enzymes to form polar metabolites with no hypnotic activity and which are rapidly eliminated.