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1. 发明申请

WO2004033484A3 USE OF STABLE GLUTAMINE DERIVATIVES TO IMPROVE DRUG ABSORPTION 审中-公开
公开(公告)号：WO2004033484A3
公开(公告)日：2004-04-22
申请号：PCT/US2003/032379
申请日：2003-10-10
申请人： UNIVERSITY OF VIRGINIA PATENT FOUNDATION , GUERRANT, Richard, L. , THIELMAN, Nathan, M. , BRITO, Gerly, Anne de Castro , LIMA, Aldo, A., M.
发明人： GUERRANT, Richard, L. , THIELMAN, Nathan, M. , BRITO, Gerly, Anne de Castro , LIMA, Aldo, A., M.
IPC分类号： A61K38/00
摘要： The present invention relates to compositions and their use to enhance the uptake of pharmaceutical agents administered to mammalian species, including humans. More particularly, the present invention is directed to the administration of glutamine and stabilized glutamine derivatives to enhance the uptake of orally administered therapeutic agents.

2. 发明申请

WO2008008704A3 INHIBITORS OF CYCLIC NUCLEOTIDE SYNTHESIS AND THEIR USE FOR THERAPY OF VARIOUS DISEASES 审中-公开
公开(公告)号：WO2008008704A3
公开(公告)日：2008-01-17
申请号：PCT/US2007/072929
申请日：2007-07-06
申请人： UNIVERSITY OF TEXAS HEALTH SCIENCE CENTER , MURAD, Ferid , KOTS, Alexander, Y. , CHOI, Byung-Kwon , GUERRANT, Richard, L.
发明人： MURAD, Ferid , KOTS, Alexander, Y. , CHOI, Byung-Kwon , GUERRANT, Richard, L.
IPC分类号： C07D471/04 , C07D471/22 , C07D487/04
摘要： We disclose a method of inhibiting activity of adenylyl cyclase or guanylyl cyclase in a mammal by administering to the mammal an amount of a composition effective to inhibit the activity, wherein the composition contains at least one compound selected from the group consisting of structural formulae (Ia) and (Ib) and salts thereof, wherein R1 is -H or has the structure -C(=O)R8; R2 is =O or has the structure -OC(=O)R9; and R3, R4, R5, R6, and R7 are each independently selected from the group consisting of -H, -NO 2 , formula (I), -halogen, -OC(=O)R9, -OR9, -OH, -R8OH, -CH 3 , -OC(=O)CH 2 Ph, formulae (II), (III), (IV), -OPh, -CF 3 , -R8, -C(=O)OR9, -Ph, -R8Ph, formulae (V), (VI), (VII), (VIII), (IX), (X), (XI), (XII), (XIII), (XIV), (XV), (XVI), (XVII), (XVIII), (XIX), (XX), and (XXI), wherein each R8 is independently a linear or branched hydrocarbon group having from 1 to 4 carbon atoms and each R9 is independently a hydrocarbon group having from 1 to 2 carbon atoms. Administering the composition can be used to treat a disease in a mammal mediated by activity of adenylyl cyclase or guanylyl cyclase and effected by a toxin produced by a pathogenic organism or to reduce cyclic AMP or cyclic GMP levels in a mammal in need of reduction thereof. The composition can also be administered to mammalian cells in vitro. The above methods of inhibiting activity of adenylyl cyclase or guanylyl cyclase and treating diseases via such inhibition can be effective without prolonged treatment, have reversible effects, have low or no toxicity, are highly potent, are unlikely to have side effects, do not act on purinergic receptors, or can negate pathogenic toxins independently of whether the pathogenic organism survives.

3. 发明申请

WO2010107736A2 BROAD SPECTRUM BENZOTHIOPHENE-NITROTHIAZOLIDE AND OTHER ANTIMICROBIALS 审中-公开
标题翻译：广泛光谱苯并噻唑和其他抗生素
公开(公告)号：WO2010107736A2
公开(公告)日：2010-09-23
申请号：PCT/US2010/027397
申请日：2010-03-16
申请人： UNIVERSITY OF VIRGINIA PATENT FOUNDATION , HOFFMAN, Paul S. , GUERRANT, Richard L. , MACDONALD, Timothy L. , BALLARD, JR., Thomas Eric
发明人： HOFFMAN, Paul S. , GUERRANT, Richard L. , MACDONALD, Timothy L. , BALLARD, JR., Thomas Eric
IPC分类号： C07D417/12 , C07D417/10 , C07D417/14
CPC分类号： C07D417/14 , A61K31/381 , A61K31/426 , A61K31/427 , A61K31/4439 , C07D277/54 , C07D277/58 , C07D333/42 , C07D333/44 , C07D409/12 , C07D417/12 , Y02A50/47 , Y02A50/473 , Y02A50/491
摘要： The invention provides novel antimicrobial chemical entities based on a nitrothiazolide backbone that exhibit antibacterial and antiparasitic action against a wide range of human pathogens. The new classes of compounds show extended action against Gram positive bacteria including MRSA drug resistant pathogens. In the Gram-positive organisms, they specifically target and functionally inhibit microbial attachment to surfaces and biofilm formation. In Gram-negative bacteria, including enteroaggregative E. coli strains, these compounds function as pilicides by inhibiting the assembly of pilin subunits into adhesive filaments. Several of these compounds show potent antimicrobial action against Gram positive bacteria, perhaps involving novel targets. Many of the benzothiophene derivatives exhibit antimicrobial activity in the low micrograms per ml range and in blocking biofilm formation in the nanomolar range; ranges considered are well within the range of utility as therapeutics.
摘要翻译：本发明提供了基于硝基噻唑烷骨架的新型抗微生物化学物质，其对广泛的人类病原体表现出抗菌和抗寄生虫作用。新类化合物对革兰氏阳性细菌（包括MRSA耐药病原体）具有延长的作用。在革兰氏阳性生物中，它们特异性靶向和功能性地抑制微生物附着于表面和生物膜形成。在包括肠聚集大肠杆菌菌株的革兰氏阴性细菌中，这些化合物通过抑制丝氨酸亚基组装成粘合剂长丝而起二硅化物的作用。这些化合物中的几种显示出对革兰氏阳性细菌的强力抗微生物作用，可能涉及新的靶标。许多苯并噻吩衍生物以低微克每毫升范围表现出抗微生物活性，并阻止纳摩尔范围内的生物膜形成; 所考虑的范围完全在作为治疗剂的效用范围内。

4. 发明申请

WO1992016843A1 IN VITRO TEST FOR LEUKOCYTES IN BODY FLUIDS 审中-公开
标题翻译：体内血液透析液体液检测
公开(公告)号：WO1992016843A1
公开(公告)日：1992-10-01
申请号：PCT/US1992002426
申请日：1992-03-20
申请人： GUERRANT, Richard, L. , REIN, Michael, F. , BARRETT, Leah, J. , ARAUJO, Valter
IPC分类号： G01N33/545
CPC分类号： G01N33/56972
摘要： An in vitro test for determining the presence of leukocytes in a body fluid or tissue sample which is sensitive to the numbers of leukocytes typically found in inflammatory processes, such as diarrheal specimens, by testing the fecal sample with an assay utilizing an antibody for lactoferrin. Additionally, the test can be used to detect low white blood cell counts as low as about 200 WBCs/ul.
摘要翻译：通过使用用于乳铁蛋白的抗体的测定来检测粪便样品，用于测定在体液或组织样品中存在白细胞的体外试验，所述体液或组织样品对炎症过程中通常发现的白细胞数量（例如腹泻标本）敏感。此外，该测试可用于检测低至约200WBC / ul的低白细胞计数。

5. 发明申请

WO2004033484A2 USE OF STABLE GLUTAMINE DERIVATIVES TO IMPROVE DRUG ABSORPTION 审中-公开
标题翻译：使用稳定的谷氨酰胺衍生物来改善药物吸收
公开(公告)号：WO2004033484A2
公开(公告)日：2004-04-22
申请号：PCT/US0332379
申请日：2003-10-10
申请人： UNIV VIRGINIA , GUERRANT RICHARD L , THIELMAN NATHAN M , BRITO GERLY ANNE DE CASTRO , LIMA ALDO A M
发明人： GUERRANT RICHARD L , THIELMAN NATHAN M , BRITO GERLY ANNE DE CASTRO , LIMA ALDO A M
IPC分类号： A61K9/00 , A61K31/198 , A61K38/02 , A61K45/06 , A61K47/18 , C07K
CPC分类号： A61K9/0053 , A61K31/00 , A61K31/198 , A61K38/02 , A61K38/05 , A61K45/06 , A61K47/183 , A61K2300/00
摘要： The present invention relates to compositions and their use to enhance the uptake of pharmaceutical agents administered to mammalian species, including humans. More particularly, the present invention is directed to the administration of glutamine and stabilized glutamine derivatives to enhance the uptake of orally administered therapeutic agents.
摘要翻译：本发明涉及组合物及其用于增强对包括人在内的哺乳动物物种施用的药剂的吸收的用途。更具体地，本发明涉及施用谷氨酰胺和稳定的谷氨酰胺衍生物以增强口服给药治疗剂的摄取。

6. 发明申请

WO2011146715A1 COMPOSITIONS AND METHODS FOR THE DELIVERY OF THERAPEUTIC PEPTIDES 审中-公开
标题翻译：用于递送治疗肽的组合物和方法
公开(公告)号：WO2011146715A1
公开(公告)日：2011-11-24
申请号：PCT/US2011/037149
申请日：2011-05-19
申请人： NORTH CAROLINA STATE UNIVERSITY , UNIVERSITY OF VIRGINIA PATENT FOUNDATION , KLAENHAMMER, Todd, R. , GUERRANT, Richard, L. , KOLLING, Glynis, L. , DURMAZ, Evelyn , TIMKO, Michael, P. , WARREN, Cirle, Alcantara
发明人： KLAENHAMMER, Todd, R. , GUERRANT, Richard, L. , KOLLING, Glynis, L. , DURMAZ, Evelyn , TIMKO, Michael, P. , WARREN, Cirle, Alcantara
IPC分类号： C07K14/195 , C07K14/315 , C07K14/335 , C12N1/06 , A23C9/00 , A23L1/03 , A61K35/74 , C07K14/00
CPC分类号： A61K38/164 , A23C9/1238 , A23L33/135 , A61K35/74 , A61K2035/11 , C12N1/06 , C12P21/02
摘要： Methods and compositions for targeted delivery of biotherapeutics are provided. The compositions comprise bile-sensitive St. thermophilus bacteria modified to release a biotherapeutic agent following bile exposure. Biotherapeutic agents released by the St. thermophilus bacteria disclosed herein include AQ and AQR rich peptides. Methods of the invention comprise administering to a subject a St. thermophilus bacterium modified to release a biotherapeutic agent following bile exposure. Administration of the St. thermophilus bacterium promotes a desired therapeutic response. The bacterium may be modified to express and release AQ or AQR rich peptides which subsequently inhibit cellular apoptosis or reduce mucosal damage. Thus, methods of the invention find use in treating or preventing a variety of gastrointestinal disorders including C. difficile infection and antibiotic-associated diarrhea.
摘要翻译：提供了用于靶向递送生物治疗剂的方法和组合物。组合物包含胆汁敏感的嗜热链球菌，其被修饰以在胆汁暴露后释放生物治疗剂。由本文公开的嗜热链球菌细菌释放的生物治疗剂包括AQ和AQR丰富的肽。本发明的方法包括向受试者施用在胆汁暴露后经修饰以释放生物治疗剂的嗜热链球菌。圣氏嗜热链霉菌的施用促进期望的治疗反应。可以修饰细菌以表达和释放富含AQ或AQR的肽，其随后抑制细胞凋亡或减少粘膜损伤。因此，本发明的方法可用于治疗或预防多种胃肠疾病，包括艰难梭菌感染和抗生素相关性腹泻。

7. 发明申请

WO2010107736A3 BROAD SPECTRUM BENZOTHIOPHENE-NITROTHIAZOLIDE AND OTHER ANTIMICROBIALS 审中-公开
标题翻译：广泛光谱苯并噻唑和其他抗生素
公开(公告)号：WO2010107736A3
公开(公告)日：2011-03-03
申请号：PCT/US2010027397
申请日：2010-03-16
申请人： UNIV VIRGINIA , HOFFMAN PAUL S , GUERRANT RICHARD L , MACDONALD TIMOTHY L , BALLARD JR THOMAS ERIC
发明人： HOFFMAN PAUL S , GUERRANT RICHARD L , MACDONALD TIMOTHY L , BALLARD JR THOMAS ERIC
IPC分类号： C07D417/12 , C07D417/10 , C07D417/14
CPC分类号： C07D417/14 , A61K31/381 , A61K31/426 , A61K31/427 , A61K31/4439 , C07D277/54 , C07D277/58 , C07D333/42 , C07D333/44 , C07D409/12 , C07D417/12
摘要： The invention provides novel antimicrobial chemical entities based on a nitrothiazolide backbone that exhibit antibacterial and antiparasitic action against a wide range of human pathogens. The new classes of compounds show extended action against Gram positive bacteria including MRSA drug resistant pathogens. In the Gram-positive organisms, they specifically target and functionally inhibit microbial attachment to surfaces and biofilm formation. In Gram-negative bacteria, including enteroaggregative E. coli strains, these compounds function as pilicides by inhibiting the assembly of pilin subunits into adhesive filaments. Several of these compounds show potent antimicrobial action against Gram positive bacteria, perhaps involving novel targets. Many of the benzothiophene derivatives exhibit antimicrobial activity in the low micrograms per ml range and in blocking biofilm formation in the nanomolar range; ranges considered are well within the range of utility as therapeutics.
摘要翻译：本发明提供了基于硝基噻唑烷骨架的新型抗微生物化学物质，其表现出针对广泛范围的人类病原体的抗细菌和抗寄生虫作用。新类化合物对革兰氏阳性细菌（包括MRSA耐药病原体）具有延长的作用。在革兰氏阳性生物中，它们特异性靶向和功能性地抑制微生物附着于表面和生物膜形成。在包括肠聚集大肠杆菌菌株的革兰氏阴性细菌中，这些化合物通过抑制丝氨酸亚基组装成粘合剂长丝而起二硅化物的作用。这些化合物中的几种显示出对抗革兰氏阳性细菌的强力抗微生物作用，可能涉及新的靶标。许多苯并噻吩衍生物以低微克/ ml范围表现出抗微生物活性，并在纳摩尔范围内阻断生物膜形成; 所考虑的范围完全在作为治疗剂的效用范围内。

8. 发明申请

WO2008124150A1 METHOD OF TREATING ENTERITIS, INTESTINAL DAMAGE, AND DIARRHEA FROM C. DIFFICILE WITH AN A2A ADENOSINE RECEPTOR AGONIST 审中-公开
标题翻译：使用A2A腺苷受体激动剂治疗胆汁酸，肠内营养不良和脱水的方法
公开(公告)号：WO2008124150A1
公开(公告)日：2008-10-16
申请号：PCT/US2008/004553
申请日：2008-04-09
申请人： GUERRANT, Richard L. , LINDEN, Joel M. , WARREN, Cirle A. , SULLIVAN, Gail W. , MACDONALD, Timothy L.
发明人： GUERRANT, Richard L. , LINDEN, Joel M. , WARREN, Cirle A. , SULLIVAN, Gail W. , MACDONALD, Timothy L.
IPC分类号： A61K31/70
CPC分类号： A61K31/70
摘要： A therapeutic method for treating intestinal damage, enteritis, diarrhea, or a combination thereof caused by a C. difficile is provided. The method includes administration to a patient in need thereof an effective amount of an A2A adenosine receptor agonist, optionally in combination with an effective amount of a stable glutamine derivative, e.g., alanyl-glutamine.
摘要翻译：提供了一种用于治疗由艰难梭菌引起的肠损伤，肠炎，腹泻或其组合的治疗方法。该方法包括向有需要的患者施用有效量的A2A腺苷受体激动剂，任选地与有效量的稳定的谷氨酰胺衍生物，例如丙氨酰 - 谷氨酰胺组合。

9. 发明申请

WO2008008704A2 INHIBITORS OF CYCLIC NUCLEOTIDE SYNTHESIS AND THEIR USE FOR THERAPY OF VARIOUS DISEASES 审中-公开
标题翻译：循环核糖体合成抑制剂及其用于各种疾病的治疗
公开(公告)号：WO2008008704A2
公开(公告)日：2008-01-17
申请号：PCT/US2007072929
申请日：2007-07-06
申请人： UNIV TEXAS HEALTH SCIENCE CT , GUERRANT RICHARD L , KOTS ALEXANDER Y , MURAD FERID , CHOI BYUNG-KWON
发明人： GUERRANT RICHARD L , KOTS ALEXANDER Y , MURAD FERID , CHOI BYUNG-KWON
IPC分类号： A61K31/519
CPC分类号： A61K31/519
摘要： We disclose a method of inhibiting activity of adenylyl cyclase or guanylyl cyclase in a mammal by administering to the mammal an amount of a composition effective to inhibit the activity, wherein the composition contains at least one compound selected from the group consisting of structural formulae (Ia) and (Ib) and salts thereof, wherein R1 is -H or has the structure -C(=O)R8; R2 is =O or has the structure -OC(=O)R9; and R3, R4, R5, R6, and R7 are each independently selected from the group consisting of -H, -NO 2 , formula (I), -halogen, -OC(=O)R9, -OR9, -OH, -R8OH, -CH 3 , -OC(=O)CH 2 Ph, formulae (II), (III), (IV), -OPh, -CF 3 , -R8, -C(=O)OR9, -Ph, -R8Ph, formulae (V), (VI), (VII), (VIII), (IX), (X), (XI), (XII), (XIII), (XIV), (XV), (XVI), (XVII), (XVIII), (XIX), (XX), and (XXI), wherein each R8 is independently a linear or branched hydrocarbon group having from 1 to 4 carbon atoms and each R9 is independently a hydrocarbon group having from 1 to 2 carbon atoms. Administering the composition can be used to treat a disease in a mammal mediated by activity of adenylyl cyclase or guanylyl cyclase and effected by a toxin produced by a pathogenic organism or to reduce cyclic AMP or cyclic GMP levels in a mammal in need of reduction thereof. The composition can also be administered to mammalian cells in vitro. The above methods of inhibiting activity of adenylyl cyclase or guanylyl cyclase and treating diseases via such inhibition can be effective without prolonged treatment, have reversible effects, have low or no toxicity, are highly potent, are unlikely to have side effects, do not act on purinergic receptors, or can negate pathogenic toxins independently of whether the pathogenic organism survives.
摘要翻译：我们公开了通过向哺乳动物施用一定量的有效抑制活性的组合物来抑制腺苷酸环化酶或鸟苷酸环化酶的活性的方法，其中组合物含有至少一种选自结构式（Ia ）和（Ib）及其盐，其中R 1是-H或具有-C（= O）R 8的结构; R2为= O或具有结构-OC（= O）R 9; 并且R 3，R 4，R 5，R 6和R 7各自独立地选自-H，-NO 2，式（I）， - 卤素，-OC（= O）R 9， -OR9，-OH，-R8OH，-CH 3，-OC（= O）CH 2 Ph，式（II），（III），（IV） -OPh，-CF 3，-R 8，-C（= O）OR 9，-Ph，-R 8 Ph，式（V），（VI），（VII），（VIII）），（X），（XIII），（XIV），（XV），（XVI），（XVII），（XVIII），（XIX），（XX）其中每个R 8独立地为具有1至4个碳原子的直链或支链烃基，并且每个R 9独立地为具有1至2个碳原子的烃基。施用组合物可用于治疗由腺苷酸环化酶或鸟苷酸环化酶的活性介导的哺乳动物疾病，并且由病原生物产生的毒素影响，或减少需要还原的哺乳动物中的环AMP或环GMP水平。组合物也可以在体外施用于哺乳动物细胞。上述抑制腺苷酸环化酶或鸟苷酸环化酶的活性和通过这种抑制作用治疗疾病的方法可以在没有延长治疗的情况下有效，具有可逆作用，具有低毒性或无毒性，高度有效，不会产生副作用，不起作用嘌呤能受体，或者可以否定致病性毒素，而不管病原菌是否存活。

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