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1. 发明申请

WO2009099650A2 TREATMENT OF BLADDER DISEASES WITH A TLR7 ACTIVATOR 审中-公开
标题翻译：用TLR7激活剂治疗刮板疾病
公开(公告)号：WO2009099650A2
公开(公告)日：2009-08-13
申请号：PCT/US2009000771
申请日：2009-02-06
申请人： CARSON DENNIS A , LEONI LORENZO M
发明人： CARSON DENNIS A , LEONI LORENZO M
IPC分类号： A61K31/437 , A61K9/107 , A61K9/127 , A61K9/16 , A61P13/10 , A61P35/00
CPC分类号： A61K31/4745 , A61K9/0034
摘要： The invention provides a method for the treatment of superficial bladder cancer and inflammatory diseases of the bladder which employs certain Toll-like Receptor (TLR)-agonists.
摘要翻译：本发明提供了一种用于治疗膀胱癌的浅表性膀胱癌和炎性疾病的方法，其采用某些Toll样受体（TLR）激动剂。

2. 发明申请

WO2006065392A2 CANCER TREATMENTS 审中-公开
标题翻译：癌症治疗
公开(公告)号：WO2006065392A2
公开(公告)日：2006-06-22
申请号：PCT/US2005040068
申请日：2005-11-04
申请人： CEPHALON INC , BENDALL HEATHER HELENE , ELLIOTT GARY T , LEONI LORENZO M , NIEMEYER CHRISTINA CAROL , MULTANI PRATIK S
发明人： BENDALL HEATHER HELENE , ELLIOTT GARY T , LEONI LORENZO M , NIEMEYER CHRISTINA CAROL , MULTANI PRATIK S
IPC分类号： A61K31/4184
CPC分类号： A61K31/4184
摘要： Methods and compositions for treating cancers characterized by death-resistant cancer cells are described. In general, such methods involve administration of a therapeutically effective amount of a compound that induces mitotic catastrophe in the some, and preferably most or all, of the cancerous cells. Methods for assessing the efficacy of such treatments are also provided.
摘要翻译：描述了用于治疗以死亡抗癌细胞为特征的癌症的方法和组合物。通常，这些方法包括施用治疗有效量的化合物，所述化合物在一些并优选大部分或全部癌细胞中诱导有丝分裂灾难。还提供了评估此类治疗效果的方法。

3. 发明申请

WO2004074325A2 COMPOSITIONS AND METHODS FOR THE DETECTION AND TREATMENT OF METHYLTHIOADENOSINE PHOSPHORYLASE DEFICIENT CANCERS 审中-公开
标题翻译：检测和治疗甲基恶二磷酸酶缺乏癌症的组合物和方法
公开(公告)号：WO2004074325A2
公开(公告)日：2004-09-02
申请号：PCT/US2004/004371
申请日：2004-02-13
申请人： SALMEDIX, INC , CARSON, Dennis, A. , LEONI, Lorenzo, M.
发明人： CARSON, Dennis, A. , LEONI, Lorenzo, M.
IPC分类号： C07K16/40
CPC分类号： G01N33/5011 , C07K16/40 , C12Q1/48 , G01N33/57407 , G01N33/57496 , G01N2333/91142
摘要： Compositions and methods involving agents that specifically bind to methylthioadenosine phosphorylase (MTAP) protein are disclosed. Illustrative compositions comprise binding agents that bind to human MTAP protein in biological samples, including embedded samples. The binding agents are useful, for example, in the detection, prognosis, and/or treatment of MTAP deficient cancers. Also disclosed are kits containing the reagents necessary for the detection of human MTAP protein in an embedded sample.
摘要翻译：公开了涉及特异性结合甲硫基腺苷磷酸化酶（MTAP）蛋白的试剂的组合物和方法。说明性组合物包含在生物样品中结合人MTAP蛋白的结合剂，包括嵌入样品。结合剂可用于例如MTAP缺陷型癌症的检测，预后和/或治疗。还公开了包含在嵌入样品中检测人类MTAP蛋白所必需的试剂的试剂盒。

4. 发明申请

WO2004026116A2 USE OF ETODOCLAC TO TREAT HYPERPLASIA 审中-公开
标题翻译：使用ETODOCLAC治疗高血压
公开(公告)号：WO2004026116A2
公开(公告)日：2004-04-01
申请号：PCT/US2003/029899
申请日：2003-09-19
申请人： THE REGENTS OF THE UNIVERSITY OF CALIFORNIA , CARSON, Dennis, A. , CORR, Mary, Patricia , LEONI, Lorenzo, M.
发明人： CARSON, Dennis, A. , CORR, Mary, Patricia , LEONI, Lorenzo, M.
IPC分类号： A61B
CPC分类号： A61K31/12 , A61K31/18 , A61K31/40 , A61K31/407 , A61K31/4745 , A61K31/496 , A61K31/50 , A61K31/56 , A61K31/675 , A61K31/7052
摘要： The present invention provides a therapeutic method to treat non-malignant diseases characterized by the excessive tissue growth, e.g., hyperplastic diseases, comprising administering to a mammal (e.g., human) afflicted with excessive tissue growth, an effective amount of a derivative of an indole compound of formula (I): wherein R 1 is lower alkyl, (hydroxy)lower alkyl, lower alkenyl, lower alkynyl, lower cycloalkyl, phenyl, benzyl or 2-thienyl; R 2 , R 3 , R 4 and R 5 are the same or different and are each hydrogen or lower alkyl; each R 6 is individually hydrogen, lower alkyl, hydroxy, (hydroxy)lower alkyl, lower alkoxy, benzyloxy, lower alkanoyloxy, nitro or halo, R 7 is hydrogen, lower alkyl or lower alkenyl, X is oxy and thio, Y is carbonyl, (CH 2 ) 1-3 , (C 1 -C 3 )alkyl(CO) , or (CH 2 ) 1-3 SO 2 ; Z is hydroxy, lower alkoxy, (C 2 -C 4 )acyloxy, N(R 8 )(R 9 ), phenylamino, (ω-(4 pyridyl)(C 2 -C 4 alkoxy), (ω-((R 8 )(R 9 ) amino)(C 2 -C 4 alkoxy), an amino acid ester of (ω-(HO)(C 2 -C 4 ))alkoxy, N(R 8 )CH(R 8 )CO 2 H, 1’-D-glucuronyloxy, SO 3 H, PO 4 H 2 , N(NO)(OH), SO 2 NH 2 , PO(OH)(NH 2 ), OCH 2 CH 2 N(CH 3 ) 3 + , or tetrazolyl; wherein R 8 and R 9 are each H, (C 1 -C 3 )alkyl or together with N are a 5- or 6-membered heterocyclic ring comprising 1-3 N(R 8 ), S or nonperoxide O; n is 0, 1, 2, or 3; wherein R 8 and R 9 are each H, (C 1 -C 3 )alkyl or together with N are a 5- or 6-membered heterocyclic ring comprising 1-3 N(R 8 ), S or nonperoxide O; each alkyl or phenyl group of R 1 , R 2 , R 3 , R 4 ,R 5 , R 6 , R 7 and Z is optionally substituted with 1, 2, or 3 (C 1 -C 4 )alkyl groups; or a pharmaceutically acceptable salt thereof.
摘要翻译：本发明提供治疗以过量组织生长为特征的非恶性疾病例如增生性疾病的治疗方法，所述方法包括向患有过度组织生长的哺乳动物（例如人）施用（I）吲哚化合物的衍生物的有效量：其中R 1是低级烷基，（羟基）低级烷基，低级烯基，低级炔基，低级环烷基，苯基，苄基或2- 噻吩; R 2，R 3，R 4和R 5相同或不同，并且各自是氢或更低的烷基; 每个R 6独立地为氢，低级烷基，羟基，（羟基）低级烷基，低级烷氧基，苄氧基，低级烷酰氧基，硝基或卤素，R 7为氢，低级烷基或低级链烯基，X是氧和硫，Y是羰基，（CH 2）1-3，（C 1 -C 4）（CO）或（CH 2）1-3 1-3 SO 2;或（CH 2）1-3 SO 2 SO 2。 Z是羟基，低级烷氧基，（C 2 -C 4）酰氧基，N（R 8）（R 9）（ω-（4-吡啶基）（C 2 -C 4烷氧基）），（ω - （（R 8））（R 9）氨基）（C 2 -C 4烷氧基）的氨基酸酯，（ω-（HO）（C N（R 8）CH（R 8）CO 2 - ， - N（R 8） 2 H，1'-D-葡糖醛酸基氧基，SO 3 H，PO 4 H 2 N，N（NO）（OH ），SO 2，NH 2，PO（OH）（NH 2），OCH 2 CH 2， 2 CH（CH 3）3 +，或四唑基;其中R 8和R 8如上所定义，（C 1 -C 3）烷基或与N一起为5或6元杂环，其包含1- 3 N（R 8），S或非过氧化物O; n为0,1,2或3;其中R 8和R 9为氢，各自为H，（C 1 -C 3）烷基或与N一起为包含1-3个N（R 5） - 的5或6元杂环， 8），S或非过氧化物 e O; R 1，R 2，R 3，R 4，R 4，R 4和R 5的每个烷基或苯基 R 5，R 7和Z任选被1,2或3个（C 1 -C 4）烷基取代， -C（= 4）烷基; 或其药学上可接受的盐。

5. 发明申请

WO2006065392A3 CANCER TREATMENTS 审中-公开
公开(公告)号：WO2006065392A3
公开(公告)日：2006-06-22
申请号：PCT/US2005/040068
申请日：2005-11-04
申请人： CEPHALON, INC. , BENDALL, Heather, Helene , ELLIOTT, Gary, T. , LEONI, Lorenzo, M. , NIEMEYER, Christina, Carol , MULTANI, Pratik, S.
发明人： BENDALL, Heather, Helene , ELLIOTT, Gary, T. , LEONI, Lorenzo, M. , NIEMEYER, Christina, Carol , MULTANI, Pratik, S.
IPC分类号： A61K31/415
摘要： Methods and compositions for treating cancers characterized by death-resistant cancer cells are described. In general, such methods involve administration of a therapeutically effective amount of a compound that induces mitotic catastrophe in the some, and preferably most or all, of the cancerous cells. Methods for assessing the efficacy of such treatments are also provided.

6. 发明申请

WO2005034944A1 COMBINATIONS OF INDOLE COMPOUNDS AND ALKYLATING AGENTS FOR THE TREATMENT OF CANCER 审中-公开
标题翻译：用于治疗癌症的单一化合物和碱性药物的组合
公开(公告)号：WO2005034944A1
公开(公告)日：2005-04-21
申请号：PCT/US2004/033270
申请日：2004-10-07
申请人： SALMEDIX, INC. , LEONI, Lorenzo, M.
发明人： LEONI, Lorenzo, M.
IPC分类号： A61K31/407
CPC分类号： A61K31/407 , A61K31/136 , A61K31/167 , A61K31/196 , A61K31/404 , A61K31/4166 , A61K31/4184 , A61K31/475 , A61K31/565 , A61K31/573 , A61K31/675 , C07D491/04 , A61K2300/00
摘要： The present invention provides methods, compositions, and medicines for treating a mammal afflicted with cancer. In particular, the invention concerns administering an effective amount of an indole compound, in combination with an alkylating agent, to a mammal afflicted with cancer.
摘要翻译：本发明提供了治疗患有癌症的哺乳动物的方法，组合物和药物。特别地，本发明涉及向患有癌症的哺乳动物施用有效量的与烷基化剂组合的吲哚化合物。

7. 发明申请

WO2004042028A2 WNT AND FRIZZLED RECEPTORS AS TARGETS FOR IMMUNOTHERAPY IN HEAD AND NECK SQUAMOUS CELL CARCINOMAS 审中-公开
标题翻译： WNT和受体受体作为头部和NECK细胞癌中的免疫治疗靶标
公开(公告)号：WO2004042028A2
公开(公告)日：2004-05-21
申请号：PCT/US2003/035026
申请日：2003-11-03
申请人： THE REGENTS OF THE UNIVERSITY OF CALIFORNIA , RHEE, Chae-Seo , MALINI, Sen , WU, Christina , LEONI, Lorenzo, M. , CORR, Maripat , CARSON, Dennis, A.
发明人： RHEE, Chae-Seo , MALINI, Sen , WU, Christina , LEONI, Lorenzo, M. , CORR, Maripat , CARSON, Dennis, A.
IPC分类号： C12N
CPC分类号： C07K16/2863 , A61K2039/505 , C07K16/22 , C07K16/3015 , C07K16/3023 , C07K16/3061 , C07K2317/73 , C12Q1/6851 , C12Q1/6886 , C12Q2600/158
摘要： This application relates to proteins involved in the Wnt/frizzled signaling pathway. More specifically, it involves the role of these proteins in proliferative disorders.
摘要翻译：本申请涉及涉及Wnt /卷曲信号通路的蛋白质。更具体地说，它涉及这些蛋白质在增殖性疾病中的作用。

8. 发明申请

WO2004012746A2 NEW USES FOR INHIBITORS OF INOSINE MONOPHOSPHATE DEHYDROGENASE 审中-公开
标题翻译：新的用于抑制单磷酸脱氢酶的药物
公开(公告)号：WO2004012746A2
公开(公告)日：2004-02-12
申请号：PCT/US2003/024325
申请日：2003-08-01
申请人： THE REGENTS OF THE UNIVERSITY OF CALIFORNIA , CARSON, Dennis, A. , LEONI, Lorenzo, M. , COTTAM, Howard, B.
发明人： CARSON, Dennis, A. , LEONI, Lorenzo, M. , COTTAM, Howard, B.
IPC分类号： A61K31/7052
CPC分类号： C07H19/24 , A61K31/136 , A61K31/198 , A61K31/4745 , A61K31/7052 , A61K31/7056 , C07H17/00 , C07H17/08 , C07H19/00 , A61K2300/00
摘要： The present invention provides methods of treating cancer using inhibitors of inosine monophosphate dehydrogenase (IMPDH). The IMPDH inhibitors are combined with compounds that inhibit cellular processes regulated by GTP or ATP. Also provided are prodrugs of the IMPDH inhibitor mizoribine and its aglycone. The prodrugs are useful in practicing the methods of the invention, including immunosuppressive therapy and treatment of cancer by prolonged administration without additional therapeutic compounds.
摘要翻译：本发明提供使用肌苷一磷酸脱氢酶（IMPDH）抑制剂治疗癌症的方法。 IMPDH抑制剂与抑制由GTP或ATP调节的细胞过程的化合物组合。还提供了IMPDH抑制剂咪佐立宾及其糖苷配基的前药。前药在实施本发明的方法中是有用的，包括免疫抑制治疗和通过长时间给药治疗癌症而无需另外的治疗化合物。

9. 发明申请

WO2003096992A3 TREATMENT OF CANCER WITH MEFLOQUIRE 审中-公开
公开(公告)号：WO2003096992A3
公开(公告)日：2003-11-27
申请号：PCT/US2003/015995
申请日：2003-05-16
申请人： THE REGENTS OF THE UNIVERSITY OF CALIFORNIA , CARSON, Dennis, A. , LEONI, Lorenzo, M. , COTTAM, Howard, B.
发明人： CARSON, Dennis, A. , LEONI, Lorenzo, M. , COTTAM, Howard, B.
IPC分类号： A61K31/47
摘要： Cancers, particularly solid tumors (e.g., breast, lung, renal, colon and ovarian cancers and melanomas) and cancers of the hematologic system, e.g., hemopoietic cancers such as leukemias, lymphomas or myelomas, are treated by administration of a therapeutically effective amount of a compound having the formula (I): (I)in which the quinoline ring is substituted by from one to three groups selected from halogen and trifluoromethyl (designated in the formula by "A"), and is optionally further substituted by one or more other moieties and R is (a) NR1R2 in which R1 and R2 are independently hydrogen or C1-C4 alkyl; (b) 2-piperidyl, (c) 2-pyridyl, and (d) 5-(ethyl or vinyl)-quinuclidin-4-yl; an enantiomer of such a compound; a pharmaceutically acceptable salts of such a compound or of an enantiomer thereof; a prodrug of such a compound or of an enantiomer thereof; a metabolite of such a compound or of an enantiomer thereof; and mixtures of two or more of the foregoing. A particularly preferred compound is mefloquine.

10. 发明申请

WO2003031587A3 USE OF STAT-6 INHIBITORS AS THERAPEUTIC AGENTS 审中-公开
公开(公告)号：WO2003031587A3
公开(公告)日：2003-04-17
申请号：PCT/US2002/032503
申请日：2002-10-09
申请人： THE REGENTS OF THE UNIVERSITY OF CALIFORNIA , CARSON, Dennis, A. , COTTAM, Howard, B. , LEONI, Lorenzo, M. , BARCHECHATH, Sylvie
发明人： CARSON, Dennis, A. , COTTAM, Howard, B. , LEONI, Lorenzo, M. , BARCHECHATH, Sylvie
IPC分类号： A61K31/519
摘要： The present invention provides A therapeutic method to enhance the efficacy of interferon treatment comprising administering to a mammal subject to interferon treatment a compound which is an antagonist of the IL-4 or IL-13 signal transduction pathway in an amount effective to enhance said efficacy. The method includes treatment of diseases such as cancer, proliferative fibrotic diseases, viral diseases, or autoimmune diseases. The invention also includes the use of chemotherapeutic agents, radiation or other treatments in conjunction with the method of the invention.

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