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71. 发明申请

WO2006055578A3 ASYMMETRIC SYNTHESIS OF (-)-AGELASTATIN A 审中-公开
公开(公告)号：WO2006055578A3
公开(公告)日：2006-05-26
申请号：PCT/US2005/041418
申请日：2005-11-16
申请人： TEMPLE UNIVERSITY - OF THE COMMONWEALTH SYSTEMS OF HIGHER EDUCATION , DAVIS, Franklin, A. , DENG, Jianghe
发明人： DAVIS, Franklin, A. , DENG, Jianghe
IPC分类号： C07D241/36 , C07D271/00 , C07D487/00 , A61K43/58 , A61K43/60 , A61K43/36 , A61K31/50 , A61K31/495 , A61K31/40
摘要： The total asymmetric synthesis of the cytotoxic marine metabolite (-)-agelastatin A (I) has been achieved from a 4,5-diamino-cyclopenten-2-one derived intermediate. This key intermediate was efficiently prepared from a sulfinimine-derived alpha-beta-diamino ester using ring closing metathesis.

72. 发明申请

WO2005123698A1 FUNGICIDES BASED ON NITROGEN-CONTAINING HETEROCYCLES 审中-公开
标题翻译：基于含氮杂质的杀真菌剂
公开(公告)号：WO2005123698A1
公开(公告)日：2005-12-29
申请号：PCT/EP2005/006687
申请日：2005-06-21
申请人： SYNGENTA PARTICIPATIONS AG , SYNGENTA LIMITED , CROWLEY, Patrick, Jelf , MÜLLER, Urs , DOBLER, Markus , WILLIAMS, John
发明人： CROWLEY, Patrick, Jelf , MÜLLER, Urs , DOBLER, Markus , WILLIAMS, John
IPC分类号： C07D241/36
CPC分类号： C07D471/04 , A01N43/90
摘要： The compound of the general formula (I), wherein W, X, Y, Z, R, R 1 and R 2 are defined as set forth in the specification, useful as fungicide.
摘要翻译：通式（I）的化合物，其中W，X，Y，Z，R，R 1和R 2定义如说明书中所述，可用作杀真菌剂。

73. 发明申请

WO2005016277A3 ARYLSULFONAMIDOBENZYLIC COMPOUNDS 审中-公开
公开(公告)号：WO2005016277A3
公开(公告)日：2005-02-24
申请号：PCT/US2004/026120
申请日：2004-08-11
申请人： AMGEN INC. , HARRISON, Martin, J. , JIAO, Xian, Yun , JONES, Stuart, D. , KAYSER, Frank , KOPECKY, David, J.
发明人： HARRISON, Martin, J. , JIAO, Xian, Yun , JONES, Stuart, D. , KAYSER, Frank , KOPECKY, David, J.
IPC分类号： C07D241/36
摘要： Compounds, pharmaceutical compositions and methods are provided that are useful in the treatment or prevention of lipid disorders, metabolic disorders and cell-proliferative diseases. In particular, the invention provides compounds which modulate the expression and/or function of proteins involved in cholesterol metabolism. The subject compounds are particularly useful in the treatment of obesity, diabetes, hypercholesterolemia, atherosclerosis and hypolipoproteinemia.

74. 发明申请

WO2004078714A3 PROCESSES FOR PREPARING IMIDAZOQUINOXALINONES, HETEROCYCLIC-SUBSTITUTED IMIDAZOPYRAZINONES, IMIDAZOUINOXALINES AND HETEROCYCLIC-SUBSTITUTED IMIDAZOPYRAZINES 审中-公开
公开(公告)号：WO2004078714A3
公开(公告)日：2004-09-16
申请号：PCT/US2004/006549
申请日：2004-03-03
申请人： BRISTOL-MYERS SQUIBB COMPANY , CHEN, Bang-Chi , SUNDEEN, Joseph, E. , BEDNARZ, Mark, S. , CHEN, Ping
发明人： CHEN, Bang-Chi , SUNDEEN, Joseph, E. , BEDNARZ, Mark, S. , CHEN, Ping
IPC分类号： C07D241/36
摘要： Novel processes for the preparation of imidazoquinoxalinones, heterocyclic-substituted imidazopyrazinones, imidazoquinoxalines and heterocyclic-substituted imidazopyrazines are described.

75. 发明申请

WO02055079A2 AZA-AND POLYAZA-NAPHTHALENYL CARBOXAMIDES USEFUL AS HIV INTEGRASE INHIBITORS 审中-公开
标题翻译：适合作为HIV整合酶抑制剂的AZA-和聚氮萘 - 甲酰胺类化合物
公开(公告)号：WO02055079A2
公开(公告)日：2002-07-18
申请号：PCT/US2001/042565
申请日：2001-10-09
IPC分类号： A61K31/4375 , A61P31/18 , A61P43/00 , C07D471/04 , A61K31/44 , A61K31/47 , A61K31/495 , A61K31/50 , A61K31/517 , A61K31/519 , A61K31/52 , A61K31/53 , C07D215/12 , C07D215/16 , C07D215/38 , C07D237/26 , C07D237/28 , C07D239/72 , C07D241/36 , C07D251/00 , C07D257/08 , C07D401/02 , C07D403/00 , C07D471/00 , C07D487/00
CPC分类号： C07D471/04
摘要： Aza- and polyaza-naphthalenyl carboxamide derivatives including certain quinoline carboxamide and naphthyridine carboxamide derivatives are described as inhibitors of HIV integrase and inhibitors of HIV replication. These compounds are useful in the prevention or treatment of infection by HIV and the treatment of AIDS, as compounds or pharmaceutically acceptable salts, or as ingredients in pharmaceutical compositions, optionally in combination with other antivirals, immunomodulators, antibiotics or vaccines. Methods of preventing, treating, or delaying the onset of AIDS and methods of preventing or treating infection by HIV are also described.
摘要翻译：本发明涉及氮杂 - 和多氮 - 萘基甲酰胺衍生物，包括某些喹啉甲酰胺和萘啶甲酰胺衍生物，其被描述为HIV整合酶抑制剂和HIV复制抑制剂。这些化合物可用于预防或治疗HIV感染和用于治疗AIDS，本身或以药学上可接受的盐的形式或作为药物组合物的成分，任选地与其他抗病毒药，免疫调节剂，抗生素或疫苗。还描述了预防，治疗或延迟AIDS发作的方法，以及预防或治疗HIV感染的方法。

76. 发明申请

WO0063296A3 CYANINE DYES AND SYNTHESIS METHODS THEREOF 审中-公开
标题翻译：氰基染料及其合成方法
公开(公告)号：WO0063296A3
公开(公告)日：2001-02-15
申请号：PCT/US0010533
申请日：2000-04-19
申请人： NEN LIFE SCIENCE PROD INC
发明人： RANDALL MALCOLM HARRY , BUZBY PHILIP RICHARD , ERICKSON THOMAS JOSEPH , TROMETER JOSEPH DAVID , MILLER JOSEPH JOHN JR , AHERN DAVID GEORGE , BOBROW MARK N
IPC分类号： G01N33/533 , A61K49/00 , C07D209/08 , C09B23/00 , C09K11/06 , C07D209/02 , C07D235/04 , C07D241/36 , C07D263/62 , C07D265/02 , C07D265/36 , C07D277/60 , C07D277/62 , C07D279/16 , C07D401/00 , C07D403/02 , C07D413/00 , C07D417/00 , C07D498/02
CPC分类号： A61K49/0021 , A61K49/0032 , A61K49/0052 , A61K49/0056 , C07D209/08
摘要： A cyanine dye having formula (II), wherein R1-R8 are each independently selected from a group consisting of hydrogen, C1-C6 alkyl group, and C0-C4 alkyl group having a hydrophilic substituent thereon. R11 and R12 are chosen to include a free or protected thiol, amine or hydroxyl substituent capable of reacting with a target molecule through a nucleophilic displacement mechanism. The dye is useful in labeling a variety of target molecules. Processes are described for synthesizing suitable heterocyclic and indole derivatives as precursors for the aforementioned cyanine dyes.
摘要翻译：具有式（II）的花青染料，其中R 1 -R 8各自独立地选自氢，C 1 -C 6烷基和在其上具有亲水性取代基的C 0 -C 4烷基。 R11和R12被选择为包括能够通过亲核置换机理与靶分子反应的游离或保护的硫醇，胺或羟基取代基。该染料可用于标记各种靶分子。描述了合成合适的杂环和吲哚衍生物作为前述花青染料的前体的方法。

77. 发明申请

WO00059497A1 PYRROLIDINE MODULATORS OF CHEMOKINE RECEPTOR ACTIVITY 审中-公开
标题翻译：氯霉素受体活性的吡咯烷酮调节剂
公开(公告)号：WO00059497A1
公开(公告)日：2000-10-12
申请号：PCT/US2000/009059
申请日：2000-04-05
IPC分类号： A61P9/10 , A61P31/18 , A61P37/06 , A61P37/08 , C07C259/06 , C07D401/06 , C07D401/14 , C07D405/14 , A61K31/165 , A61K31/215 , A61K31/24 , A61K31/40 , A61K31/4025 , A61K31/4155 , A61K31/4178 , A61K31/4192 , A61K31/4196 , A61K31/422 , A61K31/4245 , A61K31/433 , A61K31/435 , A61K31/44 , A61K31/4427 , A61K31/4439 , A61K31/444 , A61K31/445 , A61K31/454 , A61K31/4709 , A61K31/4725 , A61K31/495 , A61K31/496 , A61K31/50 , A61K31/501 , A61K31/535 , A61K31/5355 , C07C233/59 , C07C233/60 , C07C233/61 , C07C233/63 , C07C233/64 , C07C233/66 , C07C233/68 , C07C233/70 , C07C233/77 , C07C235/02 , C07C235/26 , C07C235/30 , C07C235/32 , C07C235/36 , C07C235/38 , C07C235/42 , C07C235/70 , C07D207/04 , C07D207/09 , C07D207/12 , C07D207/14 , C07D207/16 , C07D211/04 , C07D211/06 , C07D211/14 , C07D211/18 , C07D211/22 , C07D211/24 , C07D211/26 , C07D211/34 , C07D211/38 , C07D211/40 , C07D211/44 , C07D211/60 , C07D211/62 , C07D211/68 , C07D211/70 , C07D211/72 , C07D211/74 , C07D213/04 , C07D213/06 , C07D213/24 , C07D213/28 , C07D213/30 , C07D213/36 , C07D213/44 , C07D213/46 , C07D213/55 , C07D213/56 , C07D215/02 , C07D215/04 , C07D239/24 , C07D239/26 , C07D241/04 , C07D241/10 , C07D241/12 , C07D241/36 , C07D241/38 , C07D241/40 , C07D243/02 , C07D243/08 , C07D295/04 , C07D403/06 , C07D403/14 , C07D409/14 , C07D411/14 , C07D413/14 , C07D417/14 , C07D471/12 , C07D471/14 , C07D487/02 , C07D487/04 , C07F9/02 , A61K31/4532 , A61K41/47 , A61K42/427
CPC分类号： C07D401/06 , C07C259/06 , C07C2601/02 , C07C2601/04 , C07D401/14 , C07D405/14
摘要： The present invention is directed to pyrrolidine compounds of formula (I) wherein R , R , R , R , R , R and n are defined herein) which are useful as modulators of chemokine receptor activity. In particular, these compounds are useful as modulators of the chemokine receptors CCR-5 and/or CCR-3.
摘要翻译：本发明涉及式（I）的吡咯烷化合物，其中R 1，R 2，R 3，R 4，R 5，R 6和n如本文所定义），其中可用作趋化因子受体活性的调节剂。特别地，这些化合物可用作趋化因子受体CCR-5和/或CCR-3的调节剂。

78. 发明申请

WO9928304A9 PDGF RECEPTOR KINASE INHIBITORY COMPOUNDS, THEIR PREPARATION AND COMPOSITIONS 审中-公开
标题翻译： PDGF受体激酶抑制化合物，其制备和组合物
公开(公告)号：WO9928304A9
公开(公告)日：1999-09-16
申请号：PCT/US9825320
申请日：1998-11-30
申请人： YISSUM RES DEV CO , FRIEDMAN MARK M , LEVITZKI ALEXANDER , GAZIT AVIV , BANAI SHMUEL , GERTZ DAVID S , GOLOMB GERSHON
发明人： LEVITZKI ALEXANDER , GAZIT AVIV , BANAI SHMUEL , GERTZ DAVID S , GOLOMB GERSHON
IPC分类号： C07D215/20 , A61K31/275 , A61K31/403 , A61K31/404 , A61K31/4155 , A61K31/47 , A61K31/498 , A61K31/4985 , A61P9/00 , A61P9/10 , A61P11/00 , A61P11/06 , A61P13/12 , A61P29/00 , A61P35/00 , A61P43/00 , C07D209/08 , C07D209/18 , C07D241/38 , C07D241/42 , C07D403/06 , C07D409/04 , C07D487/04 , C07F17/02 , C07D241/36 , A01N43/58 , C07D471/00
CPC分类号： C07D409/04 , C07D241/42 , C07D487/04
摘要： PDGF receptor kinase inhibitory compounds of the quinoxaline family, methods for their synthesis and containment in slow release pharmaceutical preparations, and their use for treatment of proliferative malignant and non-malignant diseases or disorders by local or systemic application. A compound according to the invention includes a tyrphostin of general formula (I), wherein R1 and R2 are each independently selected from the group consisting of alkyl, alkoxy, halogen, nitro and amine and Ar is selected from the group consisting of phenyl, ferrocene, thiophene, furane, pyrrole, indole, thiazole, imidazole and pyridine.
摘要翻译：喹喔啉家族的PDGF受体激酶抑制化合物，其在缓释药物制剂中的合成和遏制的方法及其用于通过局部或全身应用治疗增殖性恶性和非恶性疾病或病症的用途。根据本发明的化合物包括通式（I）的酪氨酸磷酸酯，其中R 1和R 2各自独立地选自烷基，烷氧基，卤素，硝基和胺，Ar选自苯基，二茂铁噻吩，呋喃，吡咯，吲哚，噻唑，咪唑和吡啶。

79. 发明申请

WO98046080A1 NUCLEOPHILE SUBSTITUTED ECTEINASCIDINS AND N-OXIDE ECTEINASCIDINS 审中-公开
标题翻译：核苷酸替代天冬酰胺和N-氧化物细胞因子
公开(公告)号：WO98046080A1
公开(公告)日：1998-10-22
申请号：PCT/US1998/007340
申请日：1998-04-14
IPC分类号： A01K35/00 , A61K31/539 , A61P35/00 , C07D237/26 , C07D237/36 , C07D515/22 , A01N43/58 , C07D241/36
CPC分类号： C07D515/22
摘要： Five new nucleophile substituted ecteinascidin (Et) compounds have been isolated from extracts of Ecteinascidia turbinata. These compounds have been purified by chromatographic techniques and their structures and bioactivities have been determined. The five nucleophile substituted Et compounds have been designated herein as Et 802 (1), Et 788 (2), Et 760 (3), Et 858 (4) and Et (815) (5). Also obtained were three new N-oxide ecteinascidin compounds, which have been designated herein as Et 717 (6), Et 775 (7) and Et 789 (8). Some of these newly discovered Et compounds show exceedingly potent cytotoxicity against L1210.
摘要翻译：五种新的亲核取代的ecteinascidin（Et）化合物已从Ecteinascidia turbinata的提取物中分离出来。这些化合物已经通过色谱技术纯化，并且已经确定了它们的结构和生物活性。本文将五种亲核取代的Et化合物称为Et 802（1），Et 788（2），Et 760（3），Et 858（4）和Et（815）（5）。还获得了三种新的N-氧化物角叉菜胶化合物，其在本文中被称为Et 717（6），Et 775（7）和Et 789（8）。这些新发现的Et化合物中的一些对L1210显示出极强的细胞毒性。

80. 发明申请

WO1997003055A1 COMPOUNDS, COMPOSITIONS, AND METHODS FOR INHIBITING REPLICATION OF RETROVIRUSES AND FOR INHIBITING TUMOR PROMOTER INITIATED TRANSCRIPTION 审中-公开
标题翻译：化合物，组合物和抑制肝炎复发和抑制肿瘤促进剂启动转录的方法
公开(公告)号：WO1997003055A1
公开(公告)日：1997-01-30
申请号：PCT/US1996011699
申请日：1996-07-12
申请人： SLOAN-KETTERING INSTITUTE FOR CANCER RESEARCH , PROCHASKA, Hans, J.
发明人： SLOAN-KETTERING INSTITUTE FOR CANCER RESEARCH
IPC分类号： C07D241/36
CPC分类号： A61K31/4985 , A61K31/437 , A61K31/47 , A61K31/495 , A61K31/55 , A61K31/70 , A61K38/55 , C07D409/04 , C07D487/04 , A61K2300/00
摘要： The subject invention provides a pharmaceutical composition for inhibiting replication of a retrovirus which comprises a compound having structure (I), wherein Z1 is either C-R5 or N; wherein Z2 is N; wherein X1 and X2 are the same or different and O, S, or N-R4; and wherein R1, R2, R3, R4, and R5 are the same or different and are either hydrogen or a branched or unbranched alkyl group of from 1 to 3 carbons. The invention further comprises a pharmaceutical composition for inhibiting replication of a retrovirus which comprises a first compound which inhibits replication of the retrovirus and a second compound having the above-defined structure. Also provided are methods of inhibiting retroviral replication in a subject using the aforementioned compositions. This invention also provides a pharmaceutical composition for inhibiting tumor-promoter initiated transcription which comprises a compound having the above-defined structure. Also provided is a method for preventing the formation of tumors in a subject which comprises administering the aforementioned composition for inhibiting tumor-promoter initiated transcription.
摘要翻译：本发明提供了用于抑制逆转录病毒复制的药物组合物，其包含具有结构（I）的化合物，其中Z1是C-R5或N; 其中Z2为N; 其中X1和X2相同或不同，O，S或N-R4; 并且其中R 1，R 2，R 3，R 4和R 5相同或不同，并且是氢或具有1至3个碳的支链或非支链烷基。本发明还包括用于抑制逆转录病毒复制的药物组合物，其包含抑制逆转录病毒复制的第一化合物和具有上述结构的第二化合物。还提供了使用上述组合物抑制受试者的逆转录病毒复制的方法。本发明还提供一种用于抑制肿瘤启动子启动转录的药物组合物，其包含具有上述结构的化合物。还提供了一种用于预防受试者中肿瘤形成的方法，其包括给予上述用于抑制肿瘤启动子启动转录的组合物。

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