公开(公告)号：US07109244B2

公开(公告)日：2006-09-19

申请号：US10693174

申请日：2003-10-23

申请人： Kenneth L. Rinehart ,  Robert A. Warwick ,  Jesus Avila ,  Nancy L. Fregeau Gallagher ,  Dolores Garcia Gravalos ,  Glynn T. Faircloth

发明人： Kenneth L. Rinehart ,  Robert A. Warwick ,  Jesus Avila ,  Nancy L. Fregeau Gallagher ,  Dolores Garcia Gravalos ,  Glynn T. Faircloth

IPC分类号： A61K31/13

CPC分类号： C07C215/08 ,  A61K35/618 ,  C07B2200/07

摘要： Investigation of the activity of extracts of the clam Spisula polynyma has led to antitumor long-chain, straight-chain alkane or alkene compounds which have a 2-amino group and a 3-hydroxy group. The present invention is directed to compositions and methods comprising an isolated and purified long-chain, straight-chain 2-amino-3-hydroxyalkane, or prodrug thereof, and a pharmaceutically acceptable carrier, wherein the carbon chain in the long-chain, straight-chain 2-amino-3-hydroxyalkane is C16–C24.

摘要翻译： 研究蛤of提取物的活性已导致具有2-氨基和3-羟基的抗肿瘤长链，直链烷烃或烯烃化合物。 本发明涉及包含分离和纯化的长链，直链2-氨基-3-羟基烷烃或其前药以及药学上可接受的载体的组合物和方法，其中长链，直链 链2-氨基-3-羟基烷烃是C 16 -C 24。

公开(公告)号：US5739114A

公开(公告)日：1998-04-14

申请号：US558127

申请日：1995-11-13

申请人： Marina Gordaliza ,  Maria Angeles Castro ,  Arturo San Feliciano ,  Jose Maria Miguel del Corral ,  Maria Luisa Lopez ,  Glynn T. Faircloth

发明人： Marina Gordaliza ,  Maria Angeles Castro ,  Arturo San Feliciano ,  Jose Maria Miguel del Corral ,  Maria Luisa Lopez ,  Glynn T. Faircloth

IPC分类号： C07D231/54 ,  A61K31/34 ,  A61K31/343 ,  A61K31/415 ,  A61K31/42 ,  A61K31/423 ,  A61P37/06 ,  C07D209/60 ,  C07D261/20 ,  C07D307/92 ,  C07D491/04 ,  C07D491/056 ,  C07D493/04 ,  C07D498/04 ,  C07D307/77

CPC分类号： C07D307/92 ,  C07D209/60 ,  C07D261/20 ,  C07D491/04 ,  C07D493/04

摘要： Immunosuppressive cyclolignan derivatives are provided of formula (I) or (II): ##STR1## in which R.sup.1 is hydrogen, hydroxy, alkoxy; R.sup.2 and R.sup.3 are hydrogen, alkyl, acyl, or together R.sup.2 and R.sup.3 form a group --CHR.sup.4 --; R.sup.4 is hydrogen, alkyl, alkenyl, hydroxyalkyl, (poly)haloalkyl, aryl, acyloxyalkyl, alkoxy, carboxyalkyl, alkoxycarbonyl, carbamoyl; R.sup.5 when present is hydrogen, alkyl, alkenyl, aryl, (poly)haloalkyl, acyl, carbamoyl, or thiocarbamoyl; R.sup.6 is alkyl, hydroxyalkyl, haloalkyl, acyl, acyloxyalkyl, carboxy or alkoxycarbonyl; Ar is 3,4,5-trialkoxyphenyl or 4-hydroxy-3,5-dialkoxyphenyl; and X is nitrogen or oxygen.

摘要翻译： 免疫抑制性环链烷醇衍生物由式（I）或（II）提供：（I）或烷氧基; R2和R3是氢，烷基，酰基或一起R2和R3形成基团-CHR4-; R4是氢，烷基，烯基，羟烷基，（多）卤代烷基，芳基，酰氧基烷基，烷氧基，羧基烷基，烷氧基羰基，氨基甲酰基; 存在的R 5为氢，烷基，烯基，芳基，（多）卤代烷基，酰基，氨基甲酰基或硫代氨基甲酰基; R6是烷基，羟基烷基，卤代烷基，酰基，酰氧基烷基，羧基或烷氧基羰基; Ar为3,4,5-三烷氧基苯基或4-羟基-3,5-二烷氧基苯基; X是氮或氧。

公开(公告)号：US5298523A

公开(公告)日：1994-03-29

申请号：US990156

申请日：1992-12-14

申请人： Ross E. Longley ,  Glynn T. Faircloth

发明人： Ross E. Longley ,  Glynn T. Faircloth

IPC分类号： A61K31/35 ,  A61K31/42 ,  A61K31/695 ,  C07D413/14 ,  C07D493/04 ,  C07F7/18 ,  A01N43/32

CPC分类号： C07D413/14 ,  A61K31/35 ,  A61K31/42 ,  A61K31/695 ,  C07D493/04 ,  C07F7/1856

摘要： Mycalamide compounds are derived from marine sponges of the genus Mycale or prepared by synthetic methods. These compounds, and pharmaceutical compositions containing them as active ingredients, are useful as immunomodulatory agents.

摘要翻译： Mycalamide化合物衍生自Mycale属的海绵或通过合成方法制备。 这些化合物和含有它们作为活性成分的药物组合物可用作免疫调节剂。

公开(公告)号：US5073572A

公开(公告)日：1991-12-17

申请号：US481475

申请日：1990-02-16

申请人： Sarath P. Gunasekera ,  Glynn T. Faircloth ,  Amy E. Wright ,  Winnie C. Thompson ,  Neal Burres

发明人： Sarath P. Gunasekera ,  Glynn T. Faircloth ,  Amy E. Wright ,  Winnie C. Thompson ,  Neal Burres

IPC分类号： C07C33/048 ,  C07C69/025

CPC分类号： C07C33/048

摘要： Novel acetylenic alcohols were isolated from the known marine sponge Cribrochalina vasculum. These compounds, and derivatives thereof, are useful agents for the treatment of cancers of humans and animals. Also, these compounds and their derivatives can be used as immunosuppressive agents for humans and animals.

摘要翻译： 从已知的海绵Cribrochalina血管中分离出新的炔属醇。 这些化合物及其衍生物是治疗人和动物癌症的有用的药剂。 此外，这些化合物及其衍生物可以用作人和动物的免疫抑制剂。

公开(公告)号：US6030943A

公开(公告)日：2000-02-29

申请号：US73288

申请日：1998-05-06

申请人： William J. Crumb ,  Glynn T. Faircloth

发明人： William J. Crumb ,  Glynn T. Faircloth

IPC分类号： A61K38/00 ,  A61K31/407 ,  A61K35/56 ,  A61K38/08 ,  A61K38/15 ,  A61K45/06 ,  A61P9/04 ,  C07K5/00 ,  C07K7/00 ,  C07K16/00

CPC分类号： A61K45/06 ,  A61K31/407 ,  A61K38/08 ,  A61K38/15

摘要： This invention relates to a new use discovered for the compound known as Aplidine (dehydrodidemnin B) which has the following structure: Aplidine has been found to be a potent L-type calcium channel enhancer in the human heart. This effect makes Aplidine a very useful drug for the treatment of congestive heart failure, as well as useful for the treatment of atrial fibrillation.

摘要翻译： 本发明涉及一种被称为Aplidine（dehydrodidemnin B）的化合物发现的新用途，其具有以下结构：Aplidine已被发现是人类心脏中有效的L型钙通道增强剂。 这种作用使得Aplidine是治疗充血性心力衰竭的非常有用的药物，也可用于治疗房颤。

公开(公告)号：US06800661B1

公开(公告)日：2004-10-05

申请号：US09386724

申请日：1999-08-31

申请人： Kenneth L. Rinehart ,  Robert A. Warwick ,  Jesus Avila ,  Nancy L. Fregeau Gallagher ,  Dolores Garcia Gravalos ,  Glynn T. Faircloth

发明人： Kenneth L. Rinehart ,  Robert A. Warwick ,  Jesus Avila ,  Nancy L. Fregeau Gallagher ,  Dolores Garcia Gravalos ,  Glynn T. Faircloth

IPC分类号： A61V3113

CPC分类号： C07C215/08 ,  A61K35/618 ,  C07B2200/07

摘要： Investigation of the activity of extracts of the clam Spisula polynyma has led to antitumour long-chain, straight-chain alkane or alkene compounds which have a 2-amino group and a 3-hydroxy group.

摘要翻译： 对蛤蜊提取物的活性的研究Spisula polynyma已经导致具有2-氨基和3-羟基的抗肿瘤长链，直链烷烃或烯烃化合物。

公开(公告)号：US5556777A

公开(公告)日：1996-09-17

申请号：US118989

申请日：1993-09-09

申请人： Glynn T. Faircloth, Jr. ,  Francisco R. Millan ,  Librada M. C. Fernandez ,  Cristina A. Sarabia

发明人： Glynn T. Faircloth, Jr. ,  Francisco R. Millan ,  Librada M. C. Fernandez ,  Cristina A. Sarabia

IPC分类号： C07D405/14 ,  C12P17/16 ,  C12N1/20

CPC分类号： C07D405/14 ,  C12P17/16

摘要： The active component of the pharmaceutical composition of the present invention is a compound which has been isolated from the controlled aerobic fermentation of a marine microorganism, Agrobacterium sp. PH-103. The pharmaceutical compositions of the present invention, useful for post surgical graft tolerance, are thus directed to compositions comprising a pharmaceutically acceptable carrier, diluent or excipient, and an effective amount of the compound having the formula: ##STR1## This compound, known as Sesbanimide, is an alkaloid that has been previously been isolated from seeds and reported to be useful as an antitumor drug. Prior to the present invention however, this compound had not been isolated from any fermentation broth nor had it been determined to have immunomodulatory activity.

摘要翻译： 本发明的药物组合物的活性组分是从海洋微生物农杆菌属的受控好氧发酵中分离的化合物。 PH-103。 因此，可用于手术后移植物耐受性的本发明的药物组合物涉及包含药学上可接受的载体，稀释剂或赋形剂和有效量的具有下式的化合物的组合物：该化合物，称为Sesbanimide 是以前已经从种子中分离并据报道可用作抗肿瘤药物的生物碱。 然而，在本发明之前，该化合物没有从任何发酵液中分离，也没有确定具有免疫调节活性。