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91. 发明申请

WO0222107A3 PHARMACEUTICAL COMPOSITION HAVING MODIFIED CARRIER 审中-公开
标题翻译：具有改性载体的药物组合物
公开(公告)号：WO0222107A3
公开(公告)日：2003-01-16
申请号：PCT/US0126013
申请日：2001-09-07
申请人： UPJOHN CO , TEAGARDEN DIRK L , BRITTEN NANCY J , BROWN SCOTT A , CAPUTO JAMES F , EATON LESLIE C , HENDL ONDREJ , HUDA SYED F , KING HARRY M , MACHKOVECH SUSAN M , SCHAPAUGH RANDAL LEE , SPEAKER STANLEY M , STEELE JEAN M , SU CHING-CHIANG , URBAN TERRY R , WALDRON NIKI A , WHITMIRE MONICA L
发明人： TEAGARDEN DIRK L , BRITTEN NANCY J , BROWN SCOTT A , CAPUTO JAMES F , EATON LESLIE C , HENDL ONDREJ , HUDA SYED F , KING HARRY M , MACHKOVECH SUSAN M , SCHAPAUGH RANDAL LEE , SPEAKER STANLEY M , STEELE JEAN M , SU CHING-CHIANG , URBAN TERRY R , WALDRON NIKI A , WHITMIRE MONICA L
IPC分类号： A61K9/08 , A61K31/415 , A61K31/43 , A61K31/545 , A61K31/65 , A61K35/74 , A61K35/76 , A61K38/00 , A61K41/00 , A61K45/00 , A61K45/06 , A61K47/06 , A61K47/14 , A61K47/44 , A61P31/04 , A61K9/48 , A61K9/00 , A61K9/107 , C07D501/00
CPC分类号： A61K31/65 , A61K9/0019 , A61K31/415 , A61K31/43 , A61K31/545 , A61K45/06 , A61K47/06 , A61K47/14 , A61K47/44 , A61K2300/00
摘要： A composition comprising: (a) one or more bioactive agents; and (b) a modified liquid carrier; wherein immediately after manufacture of the composition, said composition can be administered to a host such that the one or more bioactive agents is released to the host on a sustained basis is provided.
摘要翻译：一种组合物，其包含：（a）一种或多种生物活性剂; 和（b）改性液体载体; 其中在制备组合物之后立即将所述组合物施用于宿主，使得一种或多种生物活性剂以持续的方式释放到宿主。

92. 发明申请

WO2002085402A1 METHODS AND COMPOSITIONS FOR TREATING ORAL AND EOSOPHAGEAL LESIONS 审中-公开
标题翻译：用于治疗口腔和卵巢功能的方法和组合物
公开(公告)号：WO2002085402A1
公开(公告)日：2002-10-31
申请号：PCT/US2002/012891
申请日：2002-04-24
申请人： THE GENERAL HOSPITAL CORPORATION
发明人： PODOLSKY, Daniel, K.
IPC分类号： A61K38/00
CPC分类号： A61K38/22 , A61K31/167 , A61K31/185 , A61K31/43 , A61K31/522 , A61K31/545 , A61K31/56 , A61K31/65 , A61K31/7036 , A61K31/7048 , A61K31/728 , A61K31/79 , A61K2300/00
摘要： The invention features methods and compositions for treating or preventing lesions of the upper elimentary canal, particularly oral aphthous or mucositis lesions. Intestinal trefoil peptides are administered in effeective concentrations either alone or in combination with different therapeutic agents.
摘要翻译：本发明的特征在于用于治疗或预防上消化道病变的方法和组合物，特别是口腔口疮或粘膜炎病变。肠三叶肽单独或与不同治疗剂组合施用于有效浓度。

93. 发明申请

WO02056867A2 AN EXTENDED RELEASE PHARMACEUTICAL COMPOSITION CONTAINING beta -LACTAM ANTIBIOTICS WITH IMPROVED THERAPEUTIC EFFICACY 审中-公开
标题翻译：含有改进的治疗效果的β-LACTAM抗生素的延长释放的药物组合物
公开(公告)号：WO02056867A2
公开(公告)日：2002-07-25
申请号：PCT/IN2002/000009
申请日：2002-01-18
IPC分类号： A61K9/10 , A61K9/00 , A61K9/16 , A61K9/20 , A61K9/22 , A61K9/32 , A61K9/48 , A61K9/50 , A61K9/54 , A61K31/43 , A61K31/431 , A61K31/545 , A61K31/546 , A61K47/02 , A61K47/10 , A61K47/12 , A61K47/14 , A61K47/16 , A61K47/20 , A61K47/26 , A61K47/30 , A61K47/32 , A61K47/36 , A61K47/38 , A61K47/42 , A61K47/46 , A61P31/04 , A61K9/24
CPC分类号： A61K9/0095 , A61K9/1652 , A61K9/2081 , A61K9/5042 , A61K31/43
摘要： The invention disclosed in this application relates to an extended release oral pharmaceutical composition containing at least one beta -lactam anti-biotic intended for releasing the drug over an extended period upon administration. The pharmaceutical composition is useful for maintaining the desired the therapeutic concentration of active ingredient in blood for extended time periods thus meeting the requirements for effective management of infectious diseases. The pharmaceutical composition is either in the form of a tablet, capsule or dry syrup for reconstitution at the time of administration, releasing the active ingredient as initial dose and maintenance dose at a specific rate. The invention disclosed in this application also relates to a process for formulation of an extended release pharmaceutical composition containing beta -lactam antibiotics.
摘要翻译：在本申请中公开的本发明涉及一种延长释放的口服药物组合物，其含有至少一种抗生素β-内酰胺，用于在给药后长时间释放药物。药物组合物可用于将期望的活性成分在血液中的治疗浓度保持较长时间，从而满足有效治疗感染性疾病的要求。药物组合物为片剂，胶囊或干糖浆的形式，用于在给药时重构，以特定速率释放活性成分作为初始剂量和维持剂量。本申请中公开的本发明还涉及含有β-内酰胺抗生素的延长释放药物组合物的制备方法。

94. 发明申请

WO0200165A3 AGENT FOR REVERSAL OF DRUG RESISTANCE IN MYCOBACTERIUM TUBERCULOSIS 审中-公开
标题翻译：用于逆转结核分枝杆菌耐药性的试剂
公开(公告)号：WO0200165A3
公开(公告)日：2002-06-20
申请号：PCT/IB0101136
申请日：2001-06-26
申请人： BAKULESH MAFATLAL KHAMAR
IPC分类号： A61K31/43 , A61K31/431 , A61P31/06 , A61K35/00 , A61K39/04 , A61K39/40 , C12N1/00 , C12N1/12 , C12N1/20 , C12N9/84 , C12N9/86 , C12P21/04 , C12P37/00
CPC分类号： A61K31/43 , A61K31/431
摘要： Multidrug resistance to anti-tuberculous drugs poses threat in the treatment of tuberculosis. These strains are resistant to at least two first line anti-tuberculous drugs such as INH and rifampicin. Frequently, such MDR strains show resistance to all commonly used first-line agent i.e. INH, rifamcpicin, streptomycin, ethambutol and pyrazinamide. Isoniazid is the most widely used anti-tuberculous drug. Resistance to isoniazid can occur by increased expression in inhA or by mutations that lower the enzyme's affinity to NADH. Mutations in katG, which encodes catalase peroxidase, is the most common source of resistance. Another mechanism of isoniazid resistance occurs by defects in NADH dehydrogenase (Ndh) of the respiratory chain. Increases expression of AphC has been suggested as another mechanism of INH resistance in mycobacteria. The present invention overcomes INH resistance by the use of penicillins with INH. According to present invention, penicillins when used in effective amount, reduces the MIC of INH in multi-drug resistant strains of M. tuberculosis. The improved INH sensitivity, as brought by the present invention, falls within the range which can be exploited for effective therapeutic intervention.
摘要翻译：对抗结核药物的多重耐药性对治疗结核病构成威胁。这些菌株对至少两种一线抗结核药物如INH和利福平耐药。通常，这种MDR菌株对所有常用的一线药物即INH，利福平，链霉素，乙胺丁醇和吡嗪酰胺显示出抗性。异烟肼是应用最广泛的抗结核药物。对异烟肼的耐药性可以通过增加inhA的表达或降低酶对NADH的亲和力的突变而发生。编码过氧化氢酶过氧化物酶的katG突变是最常见的抗性来源。另一种异烟肼耐药机制是由呼吸链NADH脱氢酶（Ndh）缺陷引起的。增加AphC的表达已被认为是分枝杆菌中INH抗性的另一种机制。本发明通过使用含INH的青霉素来克服INH抵抗力。根据本发明，当以有效量使用青霉素时，降低了结核分枝杆菌多重耐药菌株中INH的MIC。由本发明带来的改善的INH灵敏度落入可用于有效治疗干预的范围内。

95. 发明申请

WO02024201A1 METHOD OF TREATING AQUATIC ANIMALS WITH AN ANTIMICROBIAL AGENT AND CHELATING AGENT 审中-公开
标题翻译：用抗微生物剂和螯合剂处理水生动物的方法
公开(公告)号：WO02024201A1
公开(公告)日：2002-03-28
申请号：PCT/US2001/029312
申请日：2001-09-19
IPC分类号： A61K9/00 , A61K31/165 , A61K31/43 , A61K31/65 , A61K31/7008 , A61K31/7036 , A61K31/7048 , A61K31/70
CPC分类号： A61K31/7036 , A61K9/0017 , A61K31/165 , A61K31/43 , A61K31/65 , A61K31/7008 , A61K31/7048 , A61K2300/00
摘要： The present invention relates to novel method of reducing microbial infections, especially bacterial infections, of animals, especially of aquatic animals such as fish maintained in tanks or aquaria. The present invention provides bathing and dipping methods for reducing a microbial infection of an animal with an antibiotic solution of enhanced antimicrobial activity comprising at least one chelating agent and at least one antibiotic effective against the microbial infection. The present invention also provides a method for reducing a microbial infection of an animal comprising bathing or dipping an animal having a microbial infection in an antimicrobial solution comprising the chelating agent EDTA, and at least one antibiotic, and optionally a pH buffering agent. The immersion of the aquatic animal in the antimicrobial solution containing the EDTA, antibiotic and pH buffering agent may be repeated until the microbial burden of the animal is eliminated. The present invention further provides kits for use in administering an enhanced activity antibiotic solution.
摘要翻译：本发明涉及减少动物，特别是水生动物如维持在罐或水族箱中的鱼类的微生物感染，特别是细菌感染的新方法。本发明提供了用具有增强的抗微生物活性的抗生素溶液来减少动物的微生物感染的洗浴和浸渍方法，所述抗生素溶液包含至少一种螯合剂和至少一种有效抵抗微生物感染的抗生素。本发明还提供了一种减少动物的微生物感染的方法，包括将含有微生物感染的动物浸泡或浸渍在包含螯合剂EDTA的抗微生物溶液中，以及至少一种抗生素和任选的pH缓冲剂。可以重复将水生动物浸入含有EDTA，抗生素和pH缓冲剂的抗微生物溶液中直到消除动物的微生物负担。本发明还提供了用于施用增强活性抗生素溶液的试剂盒。

96. 发明申请

WO02022107A2 PHARMACEUTICAL COMPOSITION HAVING MODIFIED CARRIER 审中-公开
标题翻译：具有改性载体的药物组合物
公开(公告)号：WO02022107A2
公开(公告)日：2002-03-21
申请号：PCT/US2001/026013
申请日：2001-09-07
IPC分类号： A61K9/08 , A61K31/415 , A61K31/43 , A61K31/545 , A61K31/65 , A61K35/74 , A61K35/76 , A61K38/00 , A61K41/00 , A61K45/00 , A61K45/06 , A61K47/06 , A61K47/14 , A61K47/44 , A61P31/04 , A61K9/00
CPC分类号： A61K31/65 , A61K9/0019 , A61K31/415 , A61K31/43 , A61K31/545 , A61K45/06 , A61K47/06 , A61K47/14 , A61K47/44 , A61K2300/00
摘要： A composition comprising: (a) one or more bioactive agents; and (b) a modified liquid carrier; wherein immediately after manufacture of the composition, said composition can be administered to a host such that the one or more bioactive agents is released to the host on a sustained basis is provided.
摘要翻译：一种组合物，其包含：（a）一种或多种生物活性剂; 和（b）改性液体载体; 其中在制备组合物之后立即将所述组合物施用于宿主，使得一种或多种生物活性剂以持续的方式释放到宿主。

97. 发明申请

WO01058471A3 NOVEL AMINO ACID AND PEPTIDE INHIBITORS OF STAPHYLOCOCCUS VIRULENCE 审中-公开
标题翻译：新西兰氨基酸和肽抑制剂 VIRULENCE
公开(公告)号：WO01058471A3
公开(公告)日：2002-03-07
申请号：PCT/US2001/004288
申请日：2001-02-09
IPC分类号： A61K38/00 , A61K31/195 , A61K31/198 , A61K31/401 , A61K31/405 , A61K31/43 , A61K31/472 , A61K38/07 , A61K38/08 , A61K38/14 , A61P31/04 , A61P43/00 , C07D209/20 , C07K5/087 , C07K7/06 , A61K45/06 , C07C229/00
CPC分类号： A61K31/43 , A61K31/195 , A61K31/198 , A61K31/401 , A61K31/405 , A61K31/472 , A61K38/07 , A61K38/08 , A61K38/14 , A61K2300/00
摘要： Isolated synthetic modified amino acids and peptides, which inhibit the production of virulence factors in bacteria, particularly Staphylococcus , are described. The amino acids and peptides can be used in a method for treatment or prevention of Staphylococcal infections or can be integrated into a medical device to inhibit the development of infection associated with the use of such devices.
摘要翻译：描述了抑制细菌，特别是葡萄球菌中毒力因子产生的分离的合成修饰氨基酸和肽。氨基酸和肽可以用于治疗或预防葡萄球菌感染的方法中，或者可以整合到医疗装置中以抑制与使用这种装置相关的感染的发展。

98. 发明申请

WO02002095A2 COMPOSITIONS AND METHODS FOR TREATING BACTERIAL INFECTIONS 审中-公开
标题翻译：用于治疗细菌感染的组合物和方法
公开(公告)号：WO02002095A2
公开(公告)日：2002-01-10
申请号：PCT/US2001/019712
申请日：2001-06-21
IPC分类号： A61K47/04 , A61K31/422 , A61K31/43 , A61K31/495 , A61K31/496 , A61K31/535 , A61K31/5377 , A61K31/54 , A61K47/10 , A61K47/12 , A61K47/32 , A61K47/36 , A61P1/00 , A61P7/00 , A61P9/00 , A61P11/00 , A61P13/02 , A61P17/00 , A61P19/00 , A61P29/00 , A61P31/04 , A61P35/00 , A61P35/02 , A61K31/00
CPC分类号： A61K31/495 , A61K31/43 , A61K31/535 , A61K31/54 , A61K2300/00
摘要： A composition having antibacterial activity is disclosed. More particularly, a mixture of an oxazolidinone compound, sulbactam, and ampicillin active agents, demonstrating activity against resistant strains of bacteria is disclosed. Methods for using an oxazolidinone compound, sulbactam, and ampicillin to treat a bacterial infection are also described.
摘要翻译：公开了具有抗菌活性的组合物。更具体地，公开了恶唑烷酮化合物，舒巴坦和氨苄青霉素活性剂的混合物，其表现出针对抗性细菌菌株的活性。还描述了使用恶唑烷酮化合物，舒巴坦和氨苄青霉素治疗细菌感染的方法。

99. 发明申请

WO02000165A2 AGENT FOR REVERSAL OF DRUG RESISTANCE IN MYCOBACTERIUM TUBERCULOSIS 审中-公开
标题翻译：药物耐药性在MYCOBACTERIUM TUBERCULOSIS中的反应代理
公开(公告)号：WO02000165A2
公开(公告)日：2002-01-03
申请号：PCT/IB2001/001136
申请日：2001-06-26
IPC分类号： A61K31/43 , A61K31/431 , A61P31/06 , A61K
CPC分类号： A61K31/43 , A61K31/431
摘要： Multidrug resistance to anti-tuberculous drugs poses threat in the treatment of tuberculosis. These strains are resistant to at least two first line anti-tuberculous drugs such as INH and rifampicin. Frequently, such MDR strains show resistance to all commonly used first-line agent i.e. INH, rifamcpicin, streptomycin, ethambutol and pyrazinamide. Isoniazid is the most widely used anti-tuberculous drug. Resistance to isoniazid can occur by increased expression in inhA or by mutations that lower the enzyme's affinity to NADH. Mutations in katG, which encodes catalase peroxidase, is the most common source of resistance. Another mechanism of isoniazid resistance occurs by defects in NADH dehydrogenase (Ndh) of the respiratory chain. Increases expression of AphC has been suggested as another mechanism of INH resistance in mycobacteria. The present invention overcomes INH resistance by the use of penicillins with INH. According to present invention, penicillins when used in effective amount, reduces the MIC of INH in multi-drug resistant strains of M. tuberculosis. The improved INH sensitivity, as brought by the present invention, falls within the range which can be exploited for effective therapeutic intervention.
摘要翻译：抗结核药物的多药耐药对结核病的治疗构成威胁。这些菌株对至少两种一线抗结核药物如INH和利福平具有抗性。通常，这样的MDR菌株对所有常用的一线制剂即INH，利福霉素，链霉素，乙胺丁醇和吡嗪酰胺显示出抗性。异烟肼是最广泛使用的抗结核药物。对异烟肼的抗性可以通过增加inhA中的表达或降低酶对NADH的亲和力的突变而发生。编码过氧化氢酶过氧化物酶的katG的突变是最常见的抵抗来源。呼吸链的NADH脱氢酶（Ndh）缺陷发生异烟肼抗性的另一种机制。已经提出增加AphC的表达是分泌细菌中INH抗性的另一种机制。本发明通过使用青霉素与INH克服INH抗性。根据本发明，当有效量使用青霉素时，降低结核分枝杆菌多药耐药株INH的MIC。由本发明提供的改善的INH灵敏度落入可用于有效治疗干预的范围内。

100. 发明申请

WO02000163A2 THE METHOD OF TREATING DRUG RESISTANT MYCOBACTERIUM TUBERCULOSIS INFECTION 审中-公开
标题翻译：治疗耐药性结核分枝杆菌感染的方法
公开(公告)号：WO02000163A2
公开(公告)日：2002-01-03
申请号：PCT/IB2001/001132
申请日：2001-06-26
IPC分类号： A61K31/43 , A61K31/4409 , A61P31/06 , A61K
CPC分类号： A61K31/43 , A61K31/4409 , A61K2300/00
摘要： Multidrug resistance to anti-tuberculous drugs poses threat in the treatment of tuberculosis. These strains are resistant to at least tow first line anti-tuberculous drugs such as INH and rifampicin. Frequently, such MDR strains show resistance to all commonly used first-line agents i.e INH, rifampicin, streptomycin, ethambutol and pyrazinamide. Isoniazid is the most widely used anti-tuberculous drug. Resistance to isoniazid can occur by increased expression on inhA or by mutations that lower the enzyme's affinity to NADH. Mutations in katG, which encodes catalase peroxidase, is the most common source of resistance. Another mechanism of isoniazid resistance occurs by defects in NADH dehydrogenase (Ndh) of the respiratory chain. Increases expression of AhpC has been suggested as another mechanism of INH resistance in mycobacteria. The present invention provides method of treating drug resistance for Mycobacterium tuberculosis infection. According to present invention, a method is provided to employ penicillin with INH. This reduces the MIC of INH and makes resistant organisms sensitive. The level of penicillins required for reversal of INH resistance is known to be achieved and maintained by therapeutic doses of penicillins.
摘要翻译：耐抗结核病威胁与干疗法治疗疾病的抵抗至少两个主要的抗结核药物异烟肼（INH）和利福平，链霉素频繁，各种可能性乙胺丁醇和吡嗪酰胺。异烟肼是最常用的抗结核药物，对异烟肼的耐药性可能是由于增强的inhA表达或降低酶对NADH的亲和力的突变造成的。编码过氧化氢酶过氧化物酶的katG突变是抗性最常见的原因。对异烟肼耐药的其他机制可能是由于呼吸链中缺乏NADH脱氢酶（Ndh），或者如所暗示的，AhpC表达增加。本发明涉及通过使用青霉素和INH治疗结核分枝杆菌感染的药物抗性的方法，其降低INH的MIC并使生物体敏感。通过施用具有治疗效果的青霉素剂量可以实现并保持逆转对INH抗性所需的青霉素水平。

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