公开(公告)号：EP1220854A2

公开(公告)日：2002-07-10

申请号：EP00966965.6

申请日：2000-09-27

Applicant: GEORGETOWN UNIVERSITY ,  Kozikowski, Alan, P. ,  Hoepping, Wolfgang Alexander

Inventor： GEORGETOWN UNIVERSITY ,  Kozikowski, Alan, P. ,  Hoepping, Wolfgang Alexander

IPC: C07D471/18 ,  A61K31/46 ,  A61P25/00 ,  A61K51/00

CPC classification number: C07D471/18 ,  A61K51/0448 ,  C07B2200/11 ,  C40B40/00

Abstract: The present invention provides compounds, specifically novel tropane analogs, capable of acting as inhibitors of reuptake of monoamines. In preferred embodiments, these compositions are selective inhibitors of serotonin and/or norepinephrine reuptake. Also provided herein are pharmaceutical compositions comprising novel tropane analogs and a pharmaceutically acceptable carrier, and methods for treating conditions in which inhibition of reuptake of monoamines is desired. The inventive compositions as described herein are also useful for medical therapy and diagnosis.

Abstract translation: 本发明提供能够作为一元胺再摄取抑制剂的化合物，特别是新颖的托烷类似物。 在优选的实施方案中，这些组合物是血清素和/或去甲肾上腺素再摄取的选择性抑制剂。 本文还提供了包含新颖托烷类似物和药学上可接受的载体的药物组合物，以及用于治疗需要抑制单胺重摄取的病症的方法。 本文所述的本发明组合物也可用于医学治疗和诊断。

公开(公告)号：WO1998024460A1

公开(公告)日：1998-06-11

申请号：PCT/US1997023122

申请日：1997-12-04

Applicant: GEORGETOWN UNIVERSITY ,  HAN, Myun ,  LEE, Paul

Inventor： GEORGETOWN UNIVERSITY

IPC: A61K35/78

CPC classification number: A61K36/537 ,  A61K2300/00

Abstract: This invention provides extracts of Salvia species essentially consisting of that fraction from a Salvia that precipitates from aqueous solution at pH

Abstract translation: 本发明提供了基本上由pH值为3的从水溶液中沉淀的来自Salvia的级分的Salvia提取物，所述沉淀物具有如下特性： 基本上完全溶解在pH6的水溶液中，溶解度开始在约pH 4下容易观察到，所述提取物的分子量为3500道尔顿。 本发明的优选实施方案提供分子量为

公开(公告)号：WO1998021956A1

公开(公告)日：1998-05-28

申请号：PCT/US1997021474

申请日：1997-11-19

Applicant: GEORGETOWN UNIVERSITY ,  YANG, Dajun ,  WANG, Shaomeng ,  KOZIKOWSKI, Alan, P. ,  LIPPMAN, Marc, E.

Inventor： GEORGETOWN UNIVERSITY

IPC: A01N43/08

CPC classification number: A61K31/708 ,  A61K31/395 ,  A61K31/495 ,  A61K31/496 ,  A61K31/551 ,  A61K31/655 ,  A61K31/704 ,  A61K31/7076 ,  C07D498/08

Abstract: The invention provides a method of inhibiting cancer cell growth, and thereby of treating cancer comprising administering to a mammal afflicted with cancer an effective amount of the compound of formula (I), wherein the variables of R1, and R2 have the meanings defined in the specification. The present invention also provides novel compounds of formula (I) as well as novel pharmaceutical compositions and intermediates useful for preparing compounds of formula (I). The figure illustrates the structure and binding activity of compounds of the invention and some of the rifamycin analogs.

Abstract translation: 本发明提供一种抑制癌细胞生长，从而治疗癌症的方法，其中包括向患有癌症的哺乳动物施用有效量的式（I）化合物，其中R1和R2的变量具有在 规范。 本发明还提供新的式（I）化合物以及可用于制备式（I）化合物的新型药物组合物和中间体。 该图示出了本发明化合物和一些利福霉素类似物的结构和结合活性。

公开(公告)号：WO1997043268A1

公开(公告)日：1997-11-20

申请号：PCT/US1997008141

申请日：1997-05-09

Applicant: GEORGETOWN UNIVERSITY ,  KOZIKOWSKI, Alan, P. ,  MA, Dawei

Inventor： GEORGETOWN UNIVERSITY

IPC: C07D245/06

CPC classification number: C07D245/06

Abstract: Compounds of formula (I) wherein R1 is H, (C1-C5)alkyl, OR , SR , N(R )(R ), halo, NO2, NHC(O)[(C1-C4)alkyl] or NHOH; R2 is a (C5-C22) hydrocarbyl group, optionally comprising 1-3 double bonds, 1-2 triple bonds or a mixture thereof, or (C6-C12)aryl(C2-C10)alkyl, wherein the alkyl moiety optionally comprises 1-2 double bonds, 1-2 triple bonds or a mixture thereof; wherein said (C5-C22) hydrocarbyl group or said (C6-C12)aryl(C2-C10)alkyl may optionally be substituted with 1 or 2 substituents independently selected from the group consisting of halo, hydroxy, cyano, nitro, (C1-C5)alkyl, (C1-C5)alkoxy, trifluoromethyl, trifluoromethoxy, -C(=O)O(C1-C5)alkyl, and N(R )(R ); R1 and R2 together are -CH(R )-CH2-C(O)-N(R )-, -C(R )=CH-C(O)N(R )-, -C(R )=CH-N(R )- or -C(R )=CH-O-; R3 is H, OH or halo; R and R are independently H or (C1-C5)alkyl; R is a (C5-C22) hydrocarbyl group; R is H or (C1-C5)alkyl; R and R are independently hydrogen, (C1-C5)alkyl, or (C1-C5)alkanoyl, or together with the nitrogen to which they are attached are pyrrolidino, piperidino or morpholino; Z is H or (C1-C5)alkyl, and Y is H or (C1-C5)alkyl; and their pharmaceutically acceptable salts, are PKC modulators and are useful for treating i.e. cancer mammals. Also disclosed are pharmaceutical compositions comprising compounds of formula (I), processes for preparing compounds of formula (I), and intermediates useful for preparing compounds of formula (I).

Abstract translation: 其中R 1是H，（C 1 -C 5）烷基，OR a，SR a，N（R a）（R b），卤素，NO 2，NHC（O） [（C 1 -C 4）烷基]或NHOH; R2是（C5-C22）烃基，任选地包含1-3个双键，1-2个三键或其混合物，或（C 6 -C 12）芳基（C 2 -C 10）烷基，其中烷基部分任选地包含1 -2双键，1-2个三键或其混合物; 其中所述（C 5 -C 22）烃基或所述（C 6 -C 12）芳基（C 2 -C 10）烷基可任选被1或2个独立地选自卤素，羟基，氰基，硝基，（C1- C5）烷基，（C1-C5）烷氧基，三氟甲基，三氟甲氧基，-C（= O）O（C1-C5）烷基和N（​​R e）（R f） R1和R2一起是-CH（R c）-CH 2 -C（O）-N（R d） - ， - C（R c）= CH-C（O）N（R d） ） - ， - C（R c）= CH-N（R d） - 或-C（R c）= CH-O-; R3是H，OH或卤素; R a和R b独立地为H或（C 1 -C 5）烷基; R c是（C 5 -C 22）烃基; R d是H或（C 1 -C 5）烷基; R e和R f独立地是氢，（C 1 -C 5）烷基或（C 1 -C 5）烷酰基，或与它们所连接的氮一起是吡咯烷子基，哌啶子基或吗啉代; Z是H或（C1-C5）烷基，Y是H或（C1-C5）烷基; 及其药学上可接受的盐是PKC调节剂，并且可用于治疗癌症哺乳动物。 还公开了包含式（I）化合物，制备式（I）化合物的方法和可用于制备式（I）化合物的中间体的药物组合物。

公开(公告)号：WO1993013807A1

公开(公告)日：1993-07-22

申请号：PCT/US1993000007

申请日：1993-01-07

Applicant: GEORGETOWN UNIVERSITY

Inventor： GEORGETOWN UNIVERSITY ,  ZWIEBEL, James, A. ,  OJEIFO, John, O.

IPC: A61K48/00

CPC classification number: C12N5/069 ,  A61K48/00

Abstract: A method for administering genetically-engineered endothelial cells to a mammal for effecting genetic therapy, which comprises distally administering to said mammal an effective amount of genetically-engineered endothelial cells, whereby said cells migrate to one or more sites of active angiogenesis in the mammal.

Abstract translation: 一种用于向哺乳动物施用基因工程内皮细胞用于进行遗传治疗的方法，其包括向所述哺乳动物远端施用有效量的遗传工程内皮细胞，由此所述细胞迁移到哺乳动物的一个或多个活性血管发生部位。

公开(公告)号：WO1992016259A1

公开(公告)日：1992-10-01

申请号：PCT/US1992001479

申请日：1992-02-27

Applicant: IRIS MEDICAL INSTRUMENTS, INC. ,  GEORGETOWN UNIVERSITY

Inventor： IRIS MEDICAL INSTRUMENTS, INC. ,  GEORGETOWN UNIVERSITY ,  BUZAWA, David, M. ,  GAASTERLAND, Douglas, E.

IPC: A61N05/06

CPC classification number: A61F9/009 ,  A61F9/008 ,  A61F9/00821 ,  A61F2009/00868 ,  A61F2009/00891

Abstract: A fiber optic handpiece has portions formed with special contours (105) that facilitate consistent placement of the probe in an axial rather than radial orientation, thus decreasing the likelihood of incidental laser exposure to unintended structures while maintaining the intrinsically higher laser-tissue coupling efficiency of a contact technique. One particular embodiment incorporates features that permit rapid and consistent positioning (120) relative to visible landmark structures such as the limbus, thereby reducing treatment variability.

Abstract translation: 光纤手机具有形成有特殊轮廓（105）的部分，其有助于以轴向而不是径向方向一致地放置探针，从而降低了偶然的激光暴露于非预期结构的可能性，同时保持了本来更高的激光组织耦合效率 联系技术。 一个具体实施例包括允许相对于诸如角膜缘的可见的地标结构的快速和一致的定位（120）的特征，从而减少治疗变异性。

公开(公告)号：WO1990008157A1

公开(公告)日：1990-07-26

申请号：PCT/US1990000171

申请日：1990-01-17

Applicant: GEORGETOWN UNIVERSITY

Inventor： GEORGETOWN UNIVERSITY ,  TALEBIAN, Abdolhossen ,  GREEN, Dianna, C. ,  SCHEIN, Philip, S.

IPC: C07H23/00

CPC classification number: C07H23/00 ,  C07F15/0093

Abstract: Platinum compounds useful in the treatment of cancer are disclosed. Compositions containing these compounds and methods of using the same are also discussed. Compounds having formula (I) wherein n is 0 or 1 and when n is 1, R1 is H or C1-C4 alkyl, R is non-substituted higher alkyl or mono or disaccharide or a derivative of a mono or disaccharide, when n is 0, R1 is H or C1-C4 alkyl, R is H, halogen, non-substituted C1-20 alkyl, aryl, aralkyloxy, mono or disaccharide, or a derivative of a mono or disaccharide, and R2 and R3 are selected from the group consisting of hydrogen, C1-4 alkyl or R2 and R3 or R2 and R3 together are linked to adjacent carbon atoms on a four, five or six membered ring structure, or R2 and R3 together form a fused or bicyclic ring with adjacent carbon atoms, or R2 and R3 together are a substituted or unsubstituted C1-5 alkylene group; with the proviso that R and R1 cannot both be hydrogen when n = 0, or a pharmaceutically acceptable salt thereof, are particularly useful.

公开(公告)号：WO1989001785A1

公开(公告)日：1989-03-09

申请号：PCT/US1988003004

申请日：1988-09-02

Applicant: GEORGETOWN UNIVERSITY

Inventor： GEORGETOWN UNIVERSITY ,  TAYLOR, Diane, W.

IPC: A61K39/395

CPC classification number: G01N33/56905 ,  A61K39/00 ,  C07K14/445 ,  C07K16/205 ,  Y02A50/412

Abstract: Continuous hybridoma cell lines have been produced that secrete monoclonal antibodies to the PfHRP-II antigen of blood stage P.falciparum. One of these, designated MAb 87-2B2, is of the IgM isotype. MAb 87-1D6, MAb 87-1D10, MAb 87-2G12, and MAb 87-1E1 are of isotype IgG1 or IgM. The monoclonal antibodies of the present invention are well suited for use in immunometric assays for the quantitative and qualitative detection of the PfHRP-II antigen. Also disclosed are anti-idiotypic and anti anti-idiotypic antibodies to the monoclonal antibodies of the present invention. The antibodies and antigen of the present invention are useful for immunodiagnostic and immunotherapeutic treatment of P.falciparum malaria in animals, including humans.

Abstract translation: 已经产生连续杂交瘤细胞系，其分泌针对血液恶性疟原虫的PfHRP-II抗原的单克隆抗体。 其中一个，称为MAb 87-2B2，是IgM同种型。 MAb 87-1D6，MAb 87-1D10，MAb 87-2G12和MAb 87-1E1是同种型IgG1或IgM。 本发明的单克隆抗体非常适合于用于定量和定性检测PfHRP-II抗原的免疫测定。 还公开了针对本发明的单克隆抗体的抗独特型和抗独特型抗体。 本发明的抗体和抗原可用于包括人在内的动物中的恶性疟原虫的免疫诊断和免疫治疗。

公开(公告)号：WO1998024788A1

公开(公告)日：1998-06-11

申请号：PCT/US1997021706

申请日：1997-12-02

Applicant: GEORGETOWN UNIVERSITY ,  KOZIKOWSKI, Alan, P. ,  ARALDI, Gian, Luca

Inventor： GEORGETOWN UNIVERSITY

IPC: C07D451/02

CPC classification number: C07D451/02

Abstract: A compound of formula (I) wherein R1 - R6 have any of the values defined in the specification, as well as pharmaceutical compositions comprising a compound of formula (I), and methods for preparing and using compounds of formula (I) are described.

Abstract translation: 描述了其中R1-R6具有本说明书中定义的任何值的式（I）化合物，以及包含式（I）化合物的药物组合物，以及制备和使用式（I）化合物的方法。

公开(公告)号：WO1997027216A1

公开(公告)日：1997-07-31

申请号：PCT/US1997001394

申请日：1997-01-29

Applicant: GEORGETOWN UNIVERSITY ,  DAVIDSON, Eugene, A. ,  YANG, Shutong

Inventor： GEORGETOWN UNIVERSITY

IPC: C07K14/00

CPC classification number: C07K14/005 ,  A61K38/00 ,  C07K2319/02 ,  C07K2319/035 ,  C07K2319/40 ,  C12N15/62 ,  C12N2710/16622 ,  C12N2710/16722 ,  C12N2730/10122

Abstract: The present invention relates to a method for amplifying the response from a protein expressed from a recombinant vaccinia vector. The present invention may be used to amplify the intended effect of expressed proteins in any method where such expression is desired, for example, in vaccine production, vaccination and gene therapy. The present invention also relates to synthetic peptides, nucleic acid sequences, preferably DNA sequences and constructs comprising a vector linked to a DNA segment which encodes a protein containing a signal peptide at its N-terminus and an anchor sequence at its C-terminus. These expression vectors are generally useful for expressing polypeptides in a variety of animal cells.

Abstract translation: 本发明涉及一种扩增来自重组痘苗载体表达的蛋白质的应答的方法。 本发明可以用于在需要这种表达的任何方法中扩增表达的蛋白质的预期效果，例如在疫苗生产，疫苗接种和基因治疗中。 本发明还涉及合成肽，核酸序列，优选DNA序列和构建体，其包含与编码在其N-末端含有信号肽的蛋白质的DNA片段连接的载体和其C-末端的锚定序列。 这些表达载体通常可用于在多种动物细胞中表达多肽。