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1. 发明申请

WO2014151630A3 COMPOUNDS AND COMPOSITIONS FOR THE TREATMENT OF PARASITIC DISEASES 审中-公开
标题翻译：用于治疗寄生虫病的化合物和组合物
公开(公告)号：WO2014151630A3
公开(公告)日：2014-09-25
申请号：PCT/US2014/026132
申请日：2014-03-13
申请人： IRM LLC , UNIVERSITY OF WASHINGTON THROUGH ITS CENTER FOR COMMERCIALIZATION , CHATTERJEE, Arnab, Kumar , LIANG, Fang , MATHISON, Casey Jacob, Nelson , MISHRA, Pranab Kumar , MOLTENI, Valentina , NAGLE, Advait, Suresh , SUPEK, Frantisek , TAN, Liying, Jocelyn , VIDAL, Agnes , GELB, Michael, Herman , BUCKNER, Frederick, Simmons , TATIPAKA, Hari, Babu , NORCROSS, Richard, Neil , GILLESPIE, John, Robert , PENDEM, Nagendar
发明人： CHATTERJEE, Arnab, Kumar , LIANG, Fang , MATHISON, Casey Jacob, Nelson , MISHRA, Pranab Kumar , MOLTENI, Valentina , NAGLE, Advait, Suresh , SUPEK, Frantisek , TAN, Liying, Jocelyn , VIDAL, Agnes , GELB, Michael, Herman , BUCKNER, Frederick, Simmons , TATIPAKA, Hari, Babu , NORCROSS, Richard, Neil , GILLESPIE, John, Robert , PENDEM, Nagendar
IPC分类号： C07D473/00 , C07D487/04 , C07D498/04 , A61K31/437 , A61K31/4353 , A61K31/52 , A61P33/02
摘要： The present invention is related to compounds of Formula A or a pharmaceutically acceptable salt, tautomer, or stereoisomer, thereof, wherein the variables are as defined herein. The present invention further relates to pharmaceutical compositions comprising such compounds and methods of using such compounds for treating, preventing, inhibiting, ameliorating, or eradicating the pathology and/or symptomology of a disease caused by a parasite, such as Leishmaniasis, Human African Trypanosomiasis and Chagas disease.
摘要翻译：本发明涉及式A的化合物或其药学上可接受的盐，互变异构体或立体异构体，其中变量如本文所定义。本发明进一步涉及包含此类化合物的药物组合物以及使用这些化合物治疗，预防，抑制，改善或根除由寄生虫引起的疾病如利什曼病，人类非洲锥虫病和人类非洲锥虫病的病理学和/或症状学的方法南美锥虫病。

2. 发明申请

WO2003006012A1 COMPOUNDS AND METHODS FOR THE INHIBITION OF TRYPANOSOMA CRUZI 审中-公开
标题翻译：化合物和方法抑制TRYPANOSOMA CRUZ I
公开(公告)号：WO2003006012A1
公开(公告)日：2003-01-23
申请号：PCT/US2002/022195
申请日：2002-07-11
申请人： YALE UNIVERSITY , UNIVERSITY OF WASHINGTON , HAMILTON, Andrew, D. , VAN VOORHIS, Wesley, C. , YOKOYAMA, Kohei , BUCKNER, Frederick, S. , OHKANDA, Junko , GELB, Michael
发明人： HAMILTON, Andrew, D. , VAN VOORHIS, Wesley, C. , YOKOYAMA, Kohei , BUCKNER, Frederick, S. , OHKANDA, Junko , GELB, Michael
IPC分类号： A61K31/4178
CPC分类号： C07D233/64 , C07D403/12 , C07D405/12 , C07D413/12 , C07D417/12
摘要： The present invention relates to compounds according to the formula (I): Where R A is a C 1 -C 10 substituted or unsubstituted linear, branch-chained or cyclic alkyl or alkenyl group or a phenyl group according to the formula (II): R B is a C 1 -C 10 substituted or unsubstituted linear, branch-chained or cyclic alkyl or alkenyl group or a phenyl group of the formula (III): R 1 , R 2 , R 3 , R 4 , R 5 , R 6 , R 7 , R 8 , R 9 and R 10 are each independently selected from H, C 1 -C 10 (preferably a C 1 -C 4 )alkyl or alkenyl group, CF 3 , F, Cl, Br, I, CN, NO 2 , NH 2 , NHR, NRR, COR (acyl group), OR (hydroxyl or ether group), CO 2 R (carboxylic acid or ester group ), or COSR (thioester group) where R is H or a C 1 -C 10 (preferably a C 1 -C 4 )alkyl or alkenyl group, an unsubstituted or substituted aryl (preferably, phenyl) or heterocycle group, or a (IV) group, where R 3 is H, a C 1 -C 10 (preferably a C 1 -C 4 ) alkyl, alkenyl, ether or a thioether group; and R 11 and R 12 are independently selected from H or a C 1 -C 3 alkyl or alkenyl group, or a pharmaceutically acceptable salt thereof and methods for treating infections caused by protozoal, fungal and/or bacterial agents such as Trypanosoma cruzi, Mycobacterium spp., Leishmania spp., Cryptococcus spp., Aspergillus spp., Histoplasma spp., Candida spp. especially Candida albicans, Pneumocystis carinii, Trichophyton spp., Microsporum spp., Malassezia spp., Rhizopus spp., Pseudallescheria spp., Blastomyces dermatitidis and Coccidiodes spp. , among others.
摘要翻译：本发明涉及式（I）的化合物：其中R AA为C1-C10取代或未取代的直链，支链或环状烷基或链烯基或根据式（II）的苯基： R B是C 1 -C 10取代或未取代的直链，支链或环状烷基或链烯基或式（III）的苯基：R 1，R 2，R 3，R R 5，R 6，R 7，R 8，R 9和R 10各自独立地选自H，C 1 -C 10（优选C 1 -C 4）烷基或烯基，CF 3，F，Cl，Br，I，CN，NO 2，NH 2，NHR，NRR，COR（酰基），OR（羟基或醚基），CO 2 R（羧酸或酯基）（硫酯基），其中R是H或C1-C10（优选C1-C4）烷基或烯基，未取代或取代的芳基（优选苯基）或杂环基或（IV）基，其中R3是H ，C1-C10（优选C1-C4）烷基，烯基，醚或硫醚基; R 11和R 12独立地选自H或C 1 -C 3烷基或链烯基，或其药学上可接受的盐，以及用于治疗由原生动物，真菌和/或细菌药物如克氏锥虫（Trypanosoma cruzi）引起的感染的方法，分枝杆菌属（Mycobacterium spp。），利什曼原虫属（Leishmania spp。），隐球菌属（Cryptococcus spp。），曲霉属（Aspergillus spp。），组织胞浆菌（Histoplasma spp。），假丝酵母属（Candida spp。特别是白色念珠菌，卡氏肺孢子虫，毛癣菌属，微孢子虫属，马拉色氏菌属，根霉属，假花链球菌属，皮球菌属和球孢子菌属等。

3. 发明申请

WO2014151630A2 COMPOUNDS AND COMPOSITIONS FOR THE TREATMENT OF PARASITIC DISEASES 审中-公开
标题翻译：用于治疗寄生虫病的化合物和组合物
公开(公告)号：WO2014151630A2
公开(公告)日：2014-09-25
申请号：PCT/US2014026132
申请日：2014-03-13
申请人： IRM LLC , UNIV WASHINGTON CT COMMERCIALI , CHATTERJEE ARNAB KUMAR , LIANG FANG , MATHISON CASEY JACOB NELSON , MISHRA PRANAB KUMAR , MOLTENI VALENTINA , NAGLE ADVAIT SURESH , SUPEK FRANTISEK , TAN LIYING JOCELYN , VIDAL AGNES , GELB MICHAEL HERMAN , BUCKNER FREDERICK SIMMONS , TATIPAKA HARI BABU , NORCROSS RICHARD NEIL , GILLESPIE JOHN ROBERT , PENDEM NAGENDAR
发明人： CHATTERJEE ARNAB KUMAR , LIANG FANG , MATHISON CASEY JACOB NELSON , MISHRA PRANAB KUMAR , MOLTENI VALENTINA , NAGLE ADVAIT SURESH , SUPEK FRANTISEK , TAN LIYING JOCELYN , VIDAL AGNES , GELB MICHAEL HERMAN , BUCKNER FREDERICK SIMMONS , TATIPAKA HARI BABU , NORCROSS RICHARD NEIL , GILLESPIE JOHN ROBERT , PENDEM NAGENDAR
IPC分类号： C07D473/00
CPC分类号： C07D473/00 , C07D471/04 , C07D487/04 , C07D498/04
摘要： The present invention is related to compounds of Formula A or a pharmaceutically acceptable salt, tautomer, or stereoisomer, thereof, wherein the variables are as defined herein. The present invention further relates to pharmaceutical compositions comprising such compounds and methods of using such compounds for treating, preventing, inhibiting, ameliorating, or eradicating the pathology and/or symptomology of a disease caused by a parasite, such as Leishmaniasis, Human African Trypanosomiasis and Chagas disease.
摘要翻译：本发明涉及式A化合物或其药学上可接受的盐，互变异构体或立体异构体，其中变量如本文所定义。本发明还涉及包含这些化合物的药物组合物和使用这些化合物治疗，预防，抑制，改善或消除由寄生虫引起的疾病的病理和/或症状的方法，例如利什曼病，人非洲锥虫病和恰加斯病。

4. 发明申请

WO2006102159A3 COMPOUNDS AND METHODS FOR THE TREATMENT OF MALARIA AND CANCER 审中-公开
标题翻译：治疗疟疾和癌症的化合物和方法
公开(公告)号：WO2006102159A3
公开(公告)日：2007-02-15
申请号：PCT/US2006009861
申请日：2006-03-17
申请人： UNIV YALE , UNIV SOUTH FLORIDA , UNIV WASHINGTON , SEBTI SAID , HAMILTON ANDREW , BUCKNER FREDERICK , GLENN MATTHEW , VOORHIS WESLEY VAN
发明人： HAMILTON ANDREW , BUCKNER FREDERICK , GLENN MATTHEW , VOORHIS WESLEY VAN
IPC分类号： A61K38/00
CPC分类号： C07D233/24 , C07D233/42 , C07D401/12 , C07D401/14 , C07D405/14 , C07D409/12 , C07D413/14
摘要： Formula (I): Where R 1 is an optionally substituted C 3 -C 12 hydrocarbyl group (preferably a cyclic alkyl group), an optionally substituted heterocyclic group, an optionally substituted aromatic group or an optionally substituted heteroaromatic group; R is a C(O) y R' group (preferably forming an optionally substituted C 2 -C 5 acyl group), or a S(O) x R' group, where y is 0 or 1 and x is 0, 1 or 2 and R' is H or an optionally substituted C 1 -C 12 alkyl group, or R' is an optionally substituted C 5 -C 12 cycloalkyl group, an optionally substituted heterocyclic group, an optionally substituted aromatic group or an optionally substituted heteroaromatic group; R 5 , R 6 , R 7 , R 8 , R 9 and R 10 are each independently selected from H, an optionally substituted C 1 -C 12 hydrocarbyl group, including a C 5 -C 12 cycloalkyl group, an optionally substituted heterocyclic group, an optionally substituted aromatic group or an optionally substituted heteroaromatic group, or R 5 and R 6 , R 7 and R 8 or R 9 and R 10 together form a keto (C=O) group; R N is H, an optionally substituted C 1 -C 12 hydrocarbyl group, an optionally substituted heterocyclic group, an optionally substituted aromatic group, or an optionally substituted heteroaromatic group; A is Formula (II): a Formula (III): group, or a Formula (IV) or Formula (V) group, where Z is N, O or S; R a is H, a C 1 -C 12 optionally substituted hydrocarbyl group or an optionally substituted aromatic group; n is from 0 to 3; and pharmaceutically acceptable salts thereof. Compounds according to the invention are useful in one or more aspects to inhibit farnesyl transferase, or to treat malaria, neoplasia, a hyperproliferative disease state or arthritis, including rheumaroid arthritis or osteoarthritis.
摘要翻译：式（I）：其中R 1是任选取代的C 3 -C 12烃基（优选环状烷基），任选地取代的杂环基，任选取代的芳基或任选取代的杂芳基; R是C（O）n R'基团（优选形成任选取代的C 2 -C 5酰基）或S （O）x R'基团，其中y为0或1，x为0,1或2，R'为H或任选取代的C 1 -C 3烷基，或者R'是任选取代的C 5 -C 12环烷基，任选取代的杂环基，任选取代的芳族基团或任选取代的杂芳基; R 5，R 6，R 7，R 8，R 9和R 9，和 R 10各自独立地选自H，任选取代的C 1 -C 12烃基，包括C 5 - 任选取代的杂环基，任选取代的芳族基团或任选取代的杂芳族基团，或R 5和R 6， R＆lt; 7＆gt;和＆lt; 8＆gt;或R 9＆gt;和＆lt; 10＆gt;一起形成酮（C = O）组; R N是H，任选取代的C 1 -C 12烃基，任选取代的杂环基，任选取代的芳族基团，或任选取代的杂芳族基团; A是式（II）：式（III）：基团，或式（IV）或式（V）基团，其中Z是N，O或S; R a是H，C 1 -C 12 - 任选取代的烃基或任选取代的芳族基团; n为0〜3; 及其药学上可接受的盐。根据本发明的化合物在一个或多个方面可用于抑制法呢基转移酶或治疗疟疾，瘤形成，过度增生性疾病状态或关节炎，包括风湿性关节炎或骨关节炎。

5. 发明申请

WO2006102159A2 COMPOUNDS AND METHODS FOR THE TREATMENT OF MALARIA AND CANCER 审中-公开
标题翻译：治疗疟疾和癌症的化合物和方法
公开(公告)号：WO2006102159A2
公开(公告)日：2006-09-28
申请号：PCT/US2006/009861
申请日：2006-03-17
申请人： YALE UNIVERSITY , UNIVERSITY OF SOUTH FLORIDA , UNIVERSITY OF WASHINGTON , SEBTI, Said , HAMILTON, Andrew , BUCKNER, Frederick , GLENN, Matthew , VOORHIS, Wesley, Van
发明人： HAMILTON, Andrew , BUCKNER, Frederick , GLENN, Matthew , VOORHIS, Wesley, Van
IPC分类号： A61K31/59
CPC分类号： C07D233/24 , C07D233/42 , C07D401/12 , C07D401/14 , C07D405/14 , C07D409/12 , C07D413/14
摘要： Formula (I): Where R 1 is an optionally substituted C 3 -C 12 hydrocarbyl group (preferably a cyclic alkyl group), an optionally substituted heterocyclic group, an optionally substituted aromatic group or an optionally substituted heteroaromatic group; R is a C(O) y R' group (preferably forming an optionally substituted C 2 -C 5 acyl group), or a S(O) x R' group, where y is 0 or 1 and x is 0, 1 or 2 and R' is H or an optionally substituted C 1 -C 12 alkyl group, or R' is an optionally substituted C 5 -C 12 cycloalkyl group, an optionally substituted heterocyclic group, an optionally substituted aromatic group or an optionally substituted heteroaromatic group; R 5 , R 6 , R 7 , R 8 , R 9 and R 10 are each independently selected from H, an optionally substituted C 1 -C 12 hydrocarbyl group, including a C 5 -C 12 cycloalkyl group, an optionally substituted heterocyclic group, an optionally substituted aromatic group or an optionally substituted heteroaromatic group, or R 5 and R 6 , R 7 and R 8 or R 9 and R 10 together form a keto (C=O) group; R N is H, an optionally substituted C 1 -C 12 hydrocarbyl group, an optionally substituted heterocyclic group, an optionally substituted aromatic group, or an optionally substituted heteroaromatic group; A is Formula (II): a Formula (III): group, or a Formula (IV) or Formula (V) group, where Z is N, O or S; R a is H, a C 1 -C 12 optionally substituted hydrocarbyl group or an optionally substituted aromatic group; n is from 0 to 3; and pharmaceutically acceptable salts thereof. Compounds according to the invention are useful in one or more aspects to inhibit farnesyl transferase, or to treat malaria, neoplasia, a hyperproliferative disease state or arthritis, including rheumaroid arthritis or osteoarthritis.
摘要翻译：式（I）：其中R 1是任选取代的C 3 -C 12烃基（优选环状烷基），任选地取代的杂环基，任选取代的芳基或任选取代的杂芳基; R是C（O）n R'基团（优选形成任选取代的C 2 -C 5酰基）或S （O）x R'基团，其中y为0或1，x为0,1或2，R'为H或任选取代的C 1 -C 3烷基，或者R'是任选取代的C 5 -C 12环烷基，任选取代的杂环基，任选取代的芳族基团或任选取代的杂芳基; R 5，R 6，R 7，R 8，R 9和R 9，和 R 10各自独立地选自H，任选取代的C 1 -C 12烃基，包括C 5 - 任选取代的杂环基，任选取代的芳族基团或任选取代的杂芳族基团，或R 5和R 6， R＆lt; 7＆gt;和＆lt; 8＆gt;或R 9＆gt;和＆lt; 10＆gt;一起形成酮（C = O）组; R N是H，任选取代的C 1 -C 12烃基，任选取代的杂环基，任选取代的芳族基团，或任选取代的杂芳族基团; A是式（II）：式（III）：基团，或式（IV）或式（V）基团，其中Z是N，O或S; R a是H，C 1 -C 12 - 任选取代的烃基或任选取代的芳族基团; n为0〜3; 及其药学上可接受的盐。根据本发明的化合物在一个或多个方面可用于抑制法呢基转移酶或治疗疟疾，瘤形成，过度增生性疾病状态或关节炎，包括风湿性关节炎或骨关节炎。

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