公开(公告)号：US5889061A

公开(公告)日：1999-03-30

申请号：US951015

申请日：1997-10-15

申请人： Benjamin J. Frydman ,  Laurence J. Marton ,  Vendohar K. Reddy ,  Aldonia L. Valasinas ,  Donald T. Witiak

发明人： Benjamin J. Frydman ,  Laurence J. Marton ,  Vendohar K. Reddy ,  Aldonia L. Valasinas ,  Donald T. Witiak

IPC分类号： C07C211/18 ,  C07C211/22 ,  C07C211/36 ,  A61K31/13

CPC分类号： C07C211/18 ,  C07C211/22 ,  C07C211/36 ,  C07C2101/02 ,  C07C2101/04

摘要： Compounds of Formula I:E-NH-D-NH-B-A-B-NH-D-NH-E (I)wherein A is C.sub.2 -C.sub.6 alkene, C.sub.3 -C.sub.6 cycloalkyl, cycloalkenyl, or cycloaryl; B is independently a single bond, C.sub.1 -C.sub.6 alkyl alkenyl; D is independently C.sub.1 -C.sub.6 alkyl or alkenyl, or C.sub.3 -C.sub.6 cycloalkyl, cycloalkenyl, or cycloaryl; and E is independently H, C.sub.1 -C.sub.6 alkyl or alkenyl; and pharmaceutically-suitable salts thereof; a synthetic method therefor, pharmaceutical dosage forms containing one of more of these compounds, and use of these compounds in the treatment of neoplastic cell growth, are disclosed.

摘要翻译： 式Ⅰ化合物：E-NH-D-NH-B-A-B-NH-D-NH-E（Ⅰ）其中A为C2-C6烯烃，C3-C6环烷基，环烯基或环芳基; B独立地是单键，C1-C6烷基烯基; D独立地为C 1 -C 6烷基或链烯基，或C 3 -C 6环烷基，环烯基或环芳基; 且E独立地为H，C 1 -C 6烷基或链烯基; 及其药学上合适的盐; 公开了其合成方法，含有这些化合物中的一种以上的药物剂型，以及这些化合物在治疗肿瘤细胞生长中的用途。

公开(公告)号：US06392098B1

公开(公告)日：2002-05-21

申请号：US09280278

申请日：1999-03-29

申请人： Benjamin J. Frydman ,  Laurence J. Marton ,  Venodhar K. Reddy ,  Aldonia L. Valasinas ,  Donald T. Witiak

发明人： Benjamin J. Frydman ,  Laurence J. Marton ,  Venodhar K. Reddy ,  Aldonia L. Valasinas ,  Donald T. Witiak

IPC分类号： A61K3113

CPC分类号： C07C211/18 ,  C07C211/22 ,  C07C211/36 ,  C07C2601/02 ,  C07C2601/04

摘要： Compounds of Formula I: E—NH—D—NH—B—A—B—NH—D—NH—E  (I) wherein A is C2-C6 alkene, C3-C6 cycloalkyl, cycloalkenyl, or cycloaryl; B is independently a single bond, C1-C6 alkyl alkenyl; D is independently C1-C6 alkyl or alkenyl, or C3-C6 cycloalkyl, cycloalkenyl, or cycloaryl; and E is independently H, C3-C6 alkyl or alkenyl; and pharmaceutically-suitable salts thereof; a synthetic method therefor, pharmaceutical dosage forms containing one of more of these compounds, and use of these compounds in the treatment of neoplastic cell growth, are disclosed.

摘要翻译： 式I化合物：其中A是C 2 -C 6烯烃，C 3 -C 6环烷基，环烯基或环芳基; B独立地是单键，C1-C6烷基烯基; D独立地为C 1 -C 6烷基或链烯基，或C 3 -C 6环烷基，环烯基或环芳基; 且E独立地为H，C 3 -C 6烷基或链烯基; 及其药学上合适的盐; 公开了其合成方法，含有这些化合物中的一种以上的药物剂型，以及这些化合物在治疗肿瘤细胞生长中的用途。

公开(公告)号：US07026347B2

公开(公告)日：2006-04-11

申请号：US10606016

申请日：2003-06-24

申请人： Benjamin Frydman ,  Aldonia L. Valasinas ,  Venodhar K. Reddy ,  Hirak S. Basu ,  Aparajita Sarkar ,  Subhra Bhattacharya ,  Yu Wang ,  Laurence J. Marton ,  Andrei V. Blokhin

发明人： Benjamin Frydman ,  Aldonia L. Valasinas ,  Venodhar K. Reddy ,  Hirak S. Basu ,  Aparajita Sarkar ,  Subhra Bhattacharya ,  Yu Wang ,  Laurence J. Marton ,  Andrei V. Blokhin

IPC分类号： A61K31/40 ,  A61K31/555 ,  A61B5/055 ,  A61B10/00 ,  C07B47/00

CPC分类号： C07D487/22

摘要： Porphyrin-polyamine conjugate compounds are disclosed which have anticancer and antitumor effects. The porphyrin moiety selectively localizes in tumors, while the polyamine moiety serves as a cytotoxic agent. Methods of making and using the porphyrin-polyamine conjugate compounds are also disclosed.

公开(公告)号：US06982351B2

公开(公告)日：2006-01-03

申请号：US10313530

申请日：2002-12-06

申请人： Benjamin Frydman ,  Aldonia L. Valasinas ,  Andrei V. Blokhin ,  Aparajita Sarkar ,  Hirak S. Basu ,  Venodhar K. Reddy ,  Laurence J. Marton ,  Yu Wang

发明人： Benjamin Frydman ,  Aldonia L. Valasinas ,  Andrei V. Blokhin ,  Aparajita Sarkar ,  Hirak S. Basu ,  Venodhar K. Reddy ,  Laurence J. Marton ,  Yu Wang

IPC分类号： C07C211/17

CPC分类号： A61K31/132 ,  C07C211/18 ,  C07C2601/02

摘要： Conformationally restricted polyamine compounds useful in treatment of cancer and other diseases marked by abnormal cell proliferation are disclosed. Improved methods of synthesizing such compounds are also disclosed. In one method of the invention, a carbene-bearing or carbene equivalent-bearing compound is reacted with the double bond of an alkene compound to form a cyclopropyl ring as the first step in the synthesis.

公开(公告)号：US20090124832A1

公开(公告)日：2009-05-14

申请号：US12357323

申请日：2009-01-21

申请人： Benjamin Frydman ,  Linda Clifford ,  Aldonia L. Valasinas ,  Andrei V. Blokhin ,  Hirak S. Basu ,  Laurence J. Marton ,  Venodhar K. Reddy

发明人： Benjamin Frydman ,  Linda Clifford ,  Aldonia L. Valasinas ,  Andrei V. Blokhin ,  Hirak S. Basu ,  Laurence J. Marton ,  Venodhar K. Reddy

IPC分类号： C07C237/06

CPC分类号： C07C215/18 ,  C07C211/14

摘要： Oligoamine compounds with anti-cancer and anti-proliferative activity are provided, as well as methods for making and using the compounds. The compounds are shown to be active against prostate cancer cell lines and against prostate cancer tumors in mice. The compounds are also useful in treatment of breast cancer and other cancers.

摘要翻译： 提供具有抗癌和抗增殖活性的寡胺化合物，以及制备和使用该化合物的方法。 该化合物显示出对前列腺癌细胞系和抗小鼠前列腺癌肿瘤的活性。 该化合物也可用于治疗乳腺癌和其它癌症。

公开(公告)号：US07235695B2

公开(公告)日：2007-06-26

申请号：US11205341

申请日：2005-08-16

申请人： Benjamin Frydman ,  Aldonia L. Valasinas ,  Andrei V. Blokhin ,  Aparajita Sarkar ,  Hirak S. Basu ,  Venodhar K. Reddy ,  Laurence J. Marton ,  Yu Wang

发明人： Benjamin Frydman ,  Aldonia L. Valasinas ,  Andrei V. Blokhin ,  Aparajita Sarkar ,  Hirak S. Basu ,  Venodhar K. Reddy ,  Laurence J. Marton ,  Yu Wang

IPC分类号： C07C209/24 ,  C07C209/28 ,  C07C211/17

CPC分类号： A61K31/132 ,  C07C211/18 ,  C07C2601/02

摘要： Conformationally restricted polyamine compounds useful in treatment of cancer and other diseases marked by abnormal cell proliferation are disclosed. Improved methods of synthesizing such compounds are also disclosed. In one method of the invention, a carbene-bearing or carbene equivalent-bearing compound is reacted with the double bond of an alkene compound to form a cyclopropyl ring as the first step in the synthesis.

公开(公告)号：US07186825B2

公开(公告)日：2007-03-06

申请号：US10873100

申请日：2004-06-21

申请人： Benjamin Frydman ,  Laurence J. Marton ,  Venodhar K. Reddy ,  Aldonia L. Valasinas ,  Andrei V. Blokhin ,  Hirak S. Basu

发明人： Benjamin Frydman ,  Laurence J. Marton ,  Venodhar K. Reddy ,  Aldonia L. Valasinas ,  Andrei V. Blokhin ,  Hirak S. Basu

IPC分类号： C07C47/00

CPC分类号： C07C211/09 ,  A61K38/00 ,  A61K47/65 ,  C07C45/46 ,  C07C67/343 ,  C07C211/18 ,  C07C211/22 ,  C07C211/23 ,  C07C211/36 ,  C07C215/14 ,  C07C257/18 ,  C07C2601/04 ,  C07C2601/08 ,  C07D207/34 ,  C07D219/10 ,  C07D235/18 ,  C07D295/185 ,  C07D307/79 ,  C07D307/92 ,  C07D311/92 ,  C07D317/70 ,  C07D487/22 ,  C07D493/04 ,  C07K5/1013 ,  C07K7/06 ,  C07C47/575 ,  C07C69/734

摘要： Novel conformationally restricted polyamine analogs are provided, as well as compositions comprising these novel polyamine analogs. Methods of using the novel polyamine analogs in treatment of diseases such as cancer are also provided. Also provided is a method of delivering these analogs specifically to tumor cells by covalently attaching polyamine analogs to porphyrin compounds, along with novel polyamine-porphyrin covalent conjugates.

摘要翻译： 提供新颖的构象限制性多胺类似物，以及包含这些新型多胺类似物的组合物。 还提供了将新型多胺类似物用于治疗诸如癌症的疾病的方法。 还提供了通过将多胺类似物共价连接到卟啉化合物以及新型多胺 - 卟啉共价缀合物将这些类似物特异性递送至肿瘤细胞的方法。