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61. 发明申请

WO01082920A2 TREATMENT OF CONGESTIVE HEART FAILURE 审中-公开
标题翻译：治疗心绞痛失败
公开(公告)号：WO01082920A2
公开(公告)日：2001-11-08
申请号：PCT/US2001/009265
申请日：2001-03-22
IPC分类号： C07D307/52 , A61K31/341 , A61K31/55 , A61K31/635 , A61K45/06 , A61P7/10 , A61P9/00 , A61P9/04 , A61P13/00 , C07D487/04 , A61K31/00
CPC分类号： A61K31/635 , A61K31/55 , A61K2300/00
摘要： Combinations of diuretics and vasopressin antagonists are useful to slow and reverse the symptoms and process of congestive heart failure, to increase the excretion of water in the urine, and to decrease the excretion of sodium and potassium ions in urine. Preferred vasopressin antagonists have the formula (I) wherein R and R are hydrogen or lower alkyl; R , R , and R are hydrogen, halo, alkyl, alkoxy, and amino; and R is hydrogen or phenyl, and a pharmaceutically acceptable salt thereof.
摘要翻译：利尿剂和加压素拮抗剂的组合可用于减缓和逆转充血性心力衰竭的症状和过程，增加尿液中的水分排泄，并减少尿液中钠和钾离子的排泄。优选的加压素拮抗剂具有式（I），其中R和R 5是氢或低级烷基; R 1，R 2和R 3是氢，卤素，烷基，烷氧基和氨基; 和R 4是氢或苯基，及其药学上可接受的盐。

62. 发明申请

WO00057885A1 PHARMACEUTICAL EMULSIONS FOR RETROVIRAL PROTEASE INHIBITORS 审中-公开
标题翻译：替代抗体蛋白酶抑制剂的药代动力学
公开(公告)号：WO00057885A1
公开(公告)日：2000-10-05
申请号：PCT/US2000/006681
申请日：2000-03-22
IPC分类号： C07D405/12 , A61K9/107 , A61K31/4433 , A61K47/10 , A61K47/14 , A61K47/18 , A61P31/12 , A61P31/14 , A61P31/18 , A61K31/635 , A61K47/44
CPC分类号： A61K9/1075
摘要： The present invention provides an emulsion formulation with high oral bioavailability containing lecithin as an emulsifier and solubilizing agent to achieve a high loading of the pyranone compound of formula (I).
摘要翻译：本发明提供一种含有卵磷脂作为乳化剂和增溶剂的具有高口服生物利用度的乳液制剂，以实现式（I）的吡喃酮化合物的高负载量。

63. 发明申请

WO00045803A2 USE OF 5-AMINOSALICYLATES AS ANTIMICROBIAL AGENTS 审中-公开
标题翻译：作为抗微生物剂使用5-氨基苯甲酸酯
公开(公告)号：WO00045803A2
公开(公告)日：2000-08-10
申请号：PCT/US2000/002802
申请日：2000-02-04
IPC分类号： A23L3/3526 , A61K31/00 , A61K31/60 , A61K31/635 , A61P31/04
CPC分类号： A61K31/606
摘要： A method of inhibiting the growth of a bacterial species in a human or non-human vertebrate employs the antimicrobial (i.e., antibiotic) properties of 5-aminosalicylates. These antimicrobial properties are also employed in an antimicrobial method of inhibiting the growth of a bacterial species in a foodstuff and in foodstuffs containing a 5-aminosalicylate compound. Pharmaceutical compositions, foodstuffs, food containers, food-handling implements, cleansers, polishes, paints, sprays, soaps, or detergents comprise 5-aminosalicylate compounds, such as mesalamine, sulphasalazine, olsalazine, ipsalazine, salicylazobenzoic acid, balsalazide, or conjugated bile acids, including ursodeoxycholic acid-5-aminosalicylic acid. The present pharmaceutical compositions can be formulated for ingestive, colonic, or topical non-systemic delivery systems or for any systemic delivery systems. Formulation can be for human or veterinary administration. Using the method and pharmaceutical preparations the growth of bacterial species, such as Clostridium perfringens, Clostridium difficile, Clostridium botulinum, and Clostridium tetani can be inhibited.
摘要翻译：抑制人或非人脊椎动物中细菌种类生长的方法采用5-氨基水杨酸酯的抗微生物（即抗生素）特性。这些抗微生物性质也用于抑制食品中的细菌种类和含有5-氨基水杨酸酯化合物的食品中的生长的抗微生物方法。药物组合物，食品，食品容器，食品处理工具，清洁剂，抛光剂，油漆，喷雾剂，肥皂或洗涤剂包括5-氨基水杨酸酯化合物，例如美沙拉嗪，柳氮磺胺吡啶，奥沙拉嗪，茜素azine嗪，水杨基苯甲酸，巴拉嗪，或共轭胆汁酸，包括熊去氧胆酸-5-氨基水杨酸。本发明的药物组合物可以配制成用于饮食，结肠或局部非系统递送系统或用于任何系统递送系统。制剂可用于人类或兽医管理。使用该方法和药物制剂可以抑制细菌种的生长，例如产气荚膜梭菌，艰难梭菌，肉毒杆菌和破伤风梭菌。

64. 发明申请

WO00037616A1 COMPOUNDS, METHODS OF SCREENING AND METHODS OF TREATMENT FOR CENTRAL AND PERIPHERAL NERVOUS SYSTEM DISORDERS 审中-公开
标题翻译：化合物，筛选方法和中枢和外周神经系统疾病的治疗方法
公开(公告)号：WO00037616A1
公开(公告)日：2000-06-29
申请号：PCT/US1999/030806
申请日：1999-12-22
IPC分类号： C12M1/34 , A61K31/00 , A61K31/05 , A61K31/165 , A61K31/17 , A61K31/192 , A61K31/195 , A61K31/196 , A61K31/27 , A61K31/341 , A61K31/357 , A61K31/4015 , A61K31/4166 , A61K31/421 , A61K31/423 , A61K31/4535 , A61K31/513 , A61K31/515 , A61K31/53 , A61K31/55 , A61K31/551 , A61K31/5513 , A61K31/635 , A61K45/00 , A61K45/06 , A61P9/00 , A61P9/02 , A61P9/10 , A61P9/12 , A61P25/00 , A61P25/04 , A61P25/06 , A61P25/08 , A61P25/18 , A61P25/28 , A61P43/00 , C12Q1/02 , C12N9/00 , A61K31/44
CPC分类号： A61K45/06 , A61K31/00 , A61K31/192 , A61K31/196 , A61K31/341 , A61K31/635 , A61K2300/00
摘要： The present invention relates to methods and compositions for treating selected conditions of the central and peripheral nervous systems employing non-synaptic mechanisms. More specifically, one aspect of the present invention relates to methods and materials for treating seizure and seizure disorders, epilepsy, status epilepticus, migraine, spreading depression, intracranial hypertension; for treating the pathophysiological effects of head trauma, stroke, ischemia and hypoxia; for treating or protecting from the pathophysiological effects of neurotoxic agents such as ethanol; and for treating neuropsychiatric disorders and central nervous system edema by administering agents that modulate ionic concentrations and/or ionic gradients in the brain, particularly ion-dependent or cation-chloride cotransporter antagonists. Electrolyte cotransport antagonists and combinations of such compositions with other agents for treating various conditions are disclosed. The present invention also relates to methods and compositions for treating pain by administering ion-dependent cotransporter antagonists. Methods and compositions for enhancing cortical function, for example, in centers of cognition, learning and memory, by administering ion-dependant cotransporter agonists are disclosed. Methods and systems for screening drug candidate compounds for desired activities using in vitro and in vivo systems are disclosed.
摘要翻译：本发明涉及使用非突触机制治疗中枢和周围神经系统的选定病症的方法和组合物。更具体地，本发明的一个方面涉及用于治疗癫痫发作和癫痫病症，癫痫，癫痫持续状态，偏头痛，扩散性抑郁症，颅内高血压的方法和材料; 用于治疗头部创伤，中风，缺血和缺氧的病理生理作用; 用于治疗或保护神经毒素如乙醇的病理生理作用; 并且通过施用调节脑中的离子浓度和/或离子梯度的药剂，特别是离子依赖性或阳离子氯化物共转运体拮抗剂来治疗神经精神障碍和中枢神经系统水肿。公开了电解质共转运拮抗剂和这些组合物与用于治疗各种条件的其它试剂的组合。本发明还涉及通过施用离子依赖性共转运体拮抗剂来治疗疼痛的方法和组合物。公开了通过施用离子依赖的共转运体激动剂来增强皮层功能的方法和组合，例如在认知，学习和记忆的中心。公开了使用体外和体内系统筛选药物候选化合物用于所需活性的方法和系统。

65. 发明申请

WO0018384A3 ANTIVIRAL COMBINATIONS COMPRISING (S)-2-ETHYL-7-FLUORO-3-OXO-3,4-DIHYDRO-2H-QUINOXALINE-1-CARBOXYLIC ACID ISOPROPYL ESTER AND AMPRENAVIR 审中-公开
标题翻译：包含（S）-2-乙基-7-氟-3-氧代-3,4-二氢-2H-喹啉-1-羧酸异丙酯和AMPRENAVIR的抗病毒组合
公开(公告)号：WO0018384A3
公开(公告)日：2000-06-08
申请号：PCT/EP9907134
申请日：1999-09-27
申请人： GLAXO GROUP LTD , MCDADE HUGH BROWNLIE , SMILEY MARGARET LYNN , ST CLAIR MARTHA HEIDER
发明人： MCDADE HUGH BROWNLIE , SMILEY MARGARET LYNN , ST CLAIR MARTHA HEIDER
IPC分类号： A61K31/63 , A61K31/495 , A61K31/635 , A61K45/06
CPC分类号： A61K31/63 , A61K31/495 , A61K2300/00
摘要： The present invention relates to therapeutic combinations comprising (S)-2-ethyl -7-fluoro -3-oxo-3, 4-dihydro-2H- quinoxaline-1- carboxylic acid isopropyl ester and 4-amino-N-( (2 syn, 3S) -2-hydroxy-4- phenyl-3-( (S)-tetrahydrofuran -3-yloxycarbonylamino) -butyl) -N-isobutyl -benzenesulfonamide (amprenavir) or a physiologically functional derivative thereof, in particular (3S) tetrahydro-3-furanyl (1S,2R)-3-[ [(4-aminophenyl) sulfonyl] (isobutyl) amino]-1- benzyl-2- (phosphonooxy) propylcarbamate or calcium (3S) tetrahydro -3-furanyl (1S,2R)-3-[ [(4-aminophenyl) sulfonyl] (isobutyl)amino] -1-benzyl-2-( phosphonooxy) propylcarbamate. The present invention is also concerned with pharmaceutical compositions containing said combinations and their use in the treatment of HIV infections including infections with HIV mutants bearing resistance to nucleoside and/or non-nucleoside inhibitors of the replications of HIV.
摘要翻译：本发明涉及包含（S）-2-乙基-7-氟-3-氧代-3,4-二氢-2H-喹喔啉-1-甲酸异丙酯和4-氨基-N-（（2 顺式，3S）-2-羟基-4-苯基-3 - （（S） - 四氢呋喃-3-基氧基羰基氨基） - 丁基）-N-异丁基 - 苯磺酰胺（安格那威）或其生理功能衍生物，特别是（3S）（1S，2R）-3 - [[（4-氨基苯基）磺酰基]（异丁基）氨基] -1-苄基-2-（膦酰氧基）丙基氨基甲酸叔丁酯或（3S），2R）-3 - [[（4-氨基苯基）磺酰基]（异丁基）氨基] -1-苄基-2-（膦酰氧基）丙基氨基甲酸叔丁酯。本发明还涉及含有所述组合的药物组合物及其在治疗HIV感染中的用途，所述HIV感染包括具有对HIV重复的核苷和/或非核苷抑制剂具有抗性的HIV突变体的感染。

66. 发明申请

WO00004862A2 BIOENHANCED FORMULATIONS COMPRISING EPROSARTAN IN ORAL SOLID DOSAGE FORM 审中-公开
标题翻译：包含EPROSARTAN在口服固体剂型的生物制剂
公开(公告)号：WO00004862A2
公开(公告)日：2000-02-03
申请号：PCT/US1999/012396
申请日：1999-07-20
IPC分类号： A61K9/14 , A61K9/16 , A61K9/20 , A61K9/26 , A61K31/415 , A61K31/4178 , A61K31/44 , A61K31/4409 , A61K31/54 , A61K31/549 , A61K31/635 , A61K47/32 , A61P9/04 , A61P9/12 , A61P13/12 , A61P43/00 , A61K
CPC分类号： A61K31/44 , A61K9/146 , A61K9/1623 , A61K9/1635 , A61K9/2077 , A61K31/415 , A61K31/4178 , A61K31/54 , A61K31/635 , A61K2300/00
摘要： This invention relates to bioenhanced formulations comprising eprosartan or eprosartan mesylate in the amorphous form, a process for its production, compositions containing the compound and methods of using the compound to block angiotensin II receptors and to treat hypertension, congestive heart failure and renal failure.
摘要翻译：本发明涉及包含非晶形式的依普罗沙坦或甲磺酸依普罗沙坦的生物增强制剂，其制备方法，含有该化合物的组合物和使用该化合物阻断血管紧张素II受体并治疗高血压，充血性心力衰竭和肾功能衰竭的方法。

67. 发明申请

WO9955339A8 ADENOSINE A1 RECEPTOR ANTAGONIST CONTAINING COMPOSITION AND METHOD FOR RESTORING DIURETIC AND RENAL FUNCTION 审中-公开
标题翻译：含有腺苷A1受体拮抗剂的组合物和恢复DIURETIC和RENAL功能的方法
公开(公告)号：WO9955339A8
公开(公告)日：1999-12-29
申请号：PCT/US9908879
申请日：1999-04-23
申请人： BIOGEN INC , BECKMAN EVAN , SMITS GLENN
发明人： BECKMAN EVAN , SMITS GLENN
IPC分类号： A61K45/06 , A61K31/196 , A61K31/341 , A61K31/40 , A61K31/44 , A61K31/519 , A61K31/52 , A61K31/522 , A61K31/54 , A61K31/58 , A61K31/635 , A61K31/64 , A61P7/10 , A61P13/12 , A61P43/00
CPC分类号： A61K31/58 , A61K31/52 , A61K31/54 , A61K31/635 , A61K31/64 , A61K2300/00
摘要： Methods and compositions for restoring diuretic and renal function comprising adenosine A1 antagonists.
摘要翻译：包括腺苷A1拮抗剂的恢复利尿和肾功能的方法和组合物。

68. 发明申请

WO99055324A1 CCR-3 RECEPTOR ANTAGONISTS 审中-公开
标题翻译： CCR-3受体拮抗剂
公开(公告)号：WO99055324A1
公开(公告)日：1999-11-04
申请号：PCT/US1999/009182
申请日：1999-04-27
IPC分类号： C07D333/34 , A61K31/18 , A61K31/216 , A61K31/223 , A61K31/381 , A61K31/415 , A61K31/4402 , A61K31/4433 , A61K31/4436 , A61K31/47 , A61K31/63 , A61K31/635 , A61P1/00 , A61P11/02 , A61P11/06 , A61P17/00 , A61P17/04 , A61P27/02 , A61P37/08 , A61P43/00 , C07D215/36 , C07D231/06 , C07D409/04
CPC分类号： A61K31/216 , A61K31/18 , A61K31/381 , A61K31/415 , A61K31/4402 , A61K31/47 , A61K31/63 , A61K31/635
摘要： CCR-3 receptor antagonists and novel methods for their use are provided.
摘要翻译：本发明提供了CCR-3受体拮抗剂以及使用这些拮抗剂的新方法。

69. 发明申请

WO99018083A1 N,N'-(SULPHONYLDI-1, 4-PHENYLEN) BIS (N'',N''- DIMETHYLFORMAMIDIN)-1, 2,3,4-TETRAHYDRO- 6-METHYL-2, 4-DIOXO-5-PYRIMIDINSULPHONATE FOR STIMULATING CELLULAR METABOLISM AND HAVING AN IMMUNOTROPIC AND ANTI-BACTERIAL ACTIVITY AND METHOD FOR PRODUCING THE SAME 审中-公开
标题翻译： N，N' - （磺酰基-1,4-苯基）双（N“，N” - 二甲基甲酰胺）-1,2,3,4-四氢-6-甲基-2,4-二氧代-5-吡啶基磺酸盐用于刺激细胞代谢并具有免疫和抗细菌活性及其生产方法
公开(公告)号：WO99018083A1
公开(公告)日：1999-04-15
申请号：PCT/RU1998/000314
申请日：1998-10-05
IPC分类号： A61K31/513 , A61K31/53 , A61K31/635 , A61P31/08 , C07C317/40 , C07D239/60 , A61K31/505
CPC分类号： C07D239/60 , C07C317/40
摘要： The present invention relates to new biologically active chemical compounds of general formula (1) which are derived from a diaminodiphenylsulphone. These compounds are obtained by reacting equi-molecular amounts of diaminodiphenylsulphone and 6-methyluracylsulphochloride in a dimethylformamide. These compounds are practically non-toxic (LD50 = 3000 mg/kg) and are active during experiments on the leprosy and tuberculosis mycobacteria. The compounds of the present invention have an active influence on cellular exchange and can be used as agents for treating leprosy, tuberculosis as well as other immuno-deficiency conditions.
摘要翻译：本发明涉及衍生自二氨基二苯砜的通式（1）的新生物活性化合物。这些化合物通过将等分子量的二氨基二苯砜和6-甲基尿酰基氯酰氯在二甲基甲酰胺中反应而获得。这些化合物实际上是无毒的（LD50 = 3000mg / kg），并且在麻风病和结核分枝杆菌的实验中是有活性的。本发明的化合物对细胞交换具有积极的影响，可用作治疗麻风病，结核病以及其它免疫缺陷病症的药剂。

70. 发明申请

WO98057648A1 METHODS OF INCREASING THE BIOAVAILABILITY OF STABLE CRYSTAL POLYMORPHS OF A COMPOUND 审中-公开
标题翻译：增加化合物稳定性晶体聚合物生物利用度的方法
公开(公告)号：WO98057648A1
公开(公告)日：1998-12-23
申请号：PCT/US1998/012474
申请日：1998-06-16
IPC分类号： A61K9/14 , A61K31/216 , A61K31/352 , A61K31/427 , A61K31/4709 , A61K31/4725 , A61K31/496 , A61K31/513 , A61K31/551 , A61K31/635 , A61K9/51
CPC分类号： A61K31/472 , A61K9/146 , A61K31/216 , A61K31/352 , A61K31/427 , A61K31/4709 , A61K31/4725 , A61K31/496 , A61K31/513 , A61K31/5375 , A61K31/551 , A61K31/635
摘要： The present invention relates to methods of increasing the bioavailability of the most stable crystalline form of a compound. The invention also relates to particles of the most stable crystalline form of a compound having an average particle size of less than 400 nm. The invention further relates to pharmaceutical compositions comprising these particles and the use of such pharmaceutical compositions for treating diseases, such as HIV.
摘要翻译：本发明涉及增加化合物最稳定结晶形式的生物利用度的方法。本发明还涉及平均粒径小于400nm的化合物最稳定的结晶形式的颗粒。本发明进一步涉及包含这些颗粒的药物组合物以及用于治疗疾病如HIV的这种药物组合物的用途。

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