公开(公告)号：US20130039883A1

公开(公告)日：2013-02-14

申请号：US13516514

申请日：2010-12-16

Applicant: Thomas Joseph Sayers ,  Nancy Lynn Booth ,  Curtis J. Henrich ,  Alan David Brooks ,  Kirk R. Gustafson ,  Karen L. Erickson

Inventor： Thomas Joseph Sayers ,  Nancy Lynn Booth ,  Curtis J. Henrich ,  Alan David Brooks ,  Kirk R. Gustafson ,  Karen L. Erickson

IPC: A61K38/19 ,  A61P35/00 ,  A61K39/395

CPC classification number: A61K45/06 ,  A61K31/047 ,  A61K31/16 ,  A61K31/568 ,  A61K2300/00

Abstract: Disclosed is a method of enhancing the response of cancer cells in a mammal to treatment with a death receptor ligand, which method comprises contacting the cancer cells with a death receptor ligand in conjunction with an effective amount of a compound described herein, for example, a cucurbitacin (I) or a withanolide (II). Also disclosed is a method of inducing apoptosis in cancer cells in a mammal, comprising contacting the cancer cells with a compound described herein, for example, a cucurbitacin (I) or a withanolide (II) and also contacting the cancer cells with a death receptor ligand, whereby apoptosis is induced in the cancer cells.

Abstract translation: 公开了一种增强哺乳动物癌细胞对死亡受体配体治疗的反应的方法，该方法包括将癌细胞与有效量的本文所述的化合物结合使用死细胞受体配体，例如， 葫芦素（I）或己内酯（II）。 还公开了一种在哺乳动物中诱导癌细胞凋亡的方法，包括使癌细胞与本文所述的化合物例如葫芦素（I）或去甲肾上腺素（II）接触，并使癌细胞与死亡受体接触 配体，由此在癌细胞中诱导细胞凋亡。

公开(公告)号：US08278348B2

公开(公告)日：2012-10-02

申请号：US12909979

申请日：2010-10-22

Applicant: Michael R. Boyd ,  Kirk R. Gustafson

Inventor： Michael R. Boyd ,  Kirk R. Gustafson

IPC: A61K31/35 ,  A61P35/00 ,  A61P35/02 ,  A61P25/28 ,  A61P19/10 ,  A61P27/06 ,  A61P15/08 ,  A61P13/00 ,  A61P31/10 ,  A61P35/04 ,  A61P19/08

CPC classification number: C07D498/08 ,  C07D309/06

Abstract: A composition comprising a substantially purified compound of the formula: in combination with at least one additional therapeutic agent, and methods of preventing or treating cancer and a condition treatable by the inhibition of vacuolar-type (H+)-ATPase.

Abstract translation: 一种组合物，其包含基本上纯化的下式的化合物：与至少一种另外的治疗剂组合，以及预防或治疗癌症的方法以及通过抑制液泡型（H +）-ATPase可治疗的病症。

公开(公告)号：US20110034547A1

公开(公告)日：2011-02-10

申请号：US12909979

申请日：2010-10-22

Applicant: Michael R. Boyd ,  Kirk R. Gustafson

Inventor： Michael R. Boyd ,  Kirk R. Gustafson

IPC: A61K31/35 ,  A61K31/625 ,  A61P35/00 ,  A61P35/02 ,  A61P25/28 ,  A61P19/10 ,  A61P27/06 ,  A61P15/08 ,  A61P13/00 ,  A61P31/10 ,  A61P35/04 ,  A61P19/08

CPC classification number: C07D498/08 ,  C07D309/06

Abstract: A composition comprising a substantially purified compound of the formula: in combination with at least one additional therapeutic agent, and methods of preventing or treating cancer and a condition treatable by the inhibition of vacuolar-type (H+)-ATPase.

Abstract translation: 一种组合物，其包含基本上纯化的下式的化合物：与至少一种另外的治疗剂组合，以及预防或治疗癌症的方法以及通过抑制液泡型（H +）-ATP酶可治疗的病症。

公开(公告)号：US06673830B2

公开(公告)日：2004-01-06

申请号：US09887375

申请日：2001-06-22

Applicant: Michael R. Boyd ,  John H. Cardellina, II ,  Kirk R. Gustafson ,  James B. McMahon ,  Richard W. Fuller ,  Gordon M. Cragg ,  Yoel Kashman ,  Doel Soejarto

Inventor： Michael R. Boyd ,  John H. Cardellina, II ,  Kirk R. Gustafson ,  James B. McMahon ,  Richard W. Fuller ,  Gordon M. Cragg ,  Yoel Kashman ,  Doel Soejarto

IPC: A01N4316

CPC classification number: C07D493/14

Abstract: The present invention provides novel antiviral compounds, refered to as calanolides, related compounds, and their derivatives, which may be isolated from plants, or derived from compounds from plants, of the genus Calophyllum in accordance with the present inventive method. The compounds and their derivatives may be used alone or in combination with other antiviral agents in compositions, such as pharmaceutical compositions, to inhibit the growth or replication of a virus, such as a retrovirus, in particular a human immunodeficiency virus, specifically HIV-1 or HIV-2.

公开(公告)号：US08741947B2

公开(公告)日：2014-06-03

申请号：US12851691

申请日：2010-08-06

Applicant: Michael R. Boyd ,  Kirk R. Gustafson ,  Charles L. Cantrell

Inventor： Michael R. Boyd ,  Kirk R. Gustafson ,  Charles L. Cantrell

IPC: A01N43/02 ,  A61K31/335 ,  C07D309/00

CPC classification number: A61K31/395 ,  A61K31/365 ,  A61K31/7048 ,  C07D498/06 ,  C07D498/08

Abstract: The present invention provides a compound of the formula (I) or (II, wherein R1 is H, alkyl, alkenyl or aryl, R2 is H, alkyl or aryl, R3 is H, a alkyl, alkenyl or aryl, R4 and R4-R8 are independently R10, C(O)R10 or SO2R10, wherein R10 is H, alkyl, alkenyl or aryl, and R9 is R9a, C(O)R9a or SO2R9a, wherein R9a is H, alkyl, alkenyl or aryl. R9a can be unsubstituted or substituted with one or more oxo(═O), OR9b, OC(O)R9b, OSO2R9b, NHR9b, NHC(O)R9b and NHSO2R9b groups. R9b is H, alkyl, alkenyl, or aryl. R9b can be unsubstituted or substituted with one or more groups such as oxo(═O), OR9c, CO2R9c, CO2R9c and OC(O)R9c. R9c is H, or a unsubstituted or substituted alkyl, alkenyl or aryl. The present invention further provides a composition comprising at least one compound of the present invention and a pharmaceutically acceptable carrier, alone or in combination with at least one additional active agent. The present invention further provides a method of treating a condition treatable by the inhibition of vacuolar-type (H+)-ATPase and a method of treating cancer.

Abstract translation: 本发明提供式（I）或（II）化合物，其中R 1为H，烷基，烯基或芳基，R 2为H，烷基或芳基，R 3为H，烷基，烯基或芳基，R 4和R 4 - R8独立地为R10，C（O）R10或SO2R10，其中R10为H，烷基，烯基或芳基，R9为R9a，C（O）R9a或SO2R9a，其中R9a为H，烷基，烯基或芳基。 被取代或被一个或多个氧代（= O），OR 9 b，OC（O）R 9b，OSO 2 R 9 b，NHR 9 b，NHC（O）R 9b和NHSO 2 R 9 b基团取代的R 9b是氢，烷基，链烯基或芳基。 或被一个或多个基团取代，例如氧代（= O），OR 9c，CO 2 R 9c，CO 2 R 9c和OC（O）R 9c。R9c是H或未取代或取代的烷基，烯基或芳基，本发明还提供一种组合物， 本发明的至少一种化合物和药学上可接受的载体，单独或与至少一种另外的活性剂组合。本发明还提供一种治疗可治疗的疾病的方法， 抑制液泡型（H +） - ATPase和一种治疗癌症的方法。

公开(公告)号：US20110190240A1

公开(公告)日：2011-08-04

申请号：US13120044

申请日：2009-09-22

Applicant: Curtis J. Henrich ,  Moon-Il Kang ,  Heidi R. Bokesch ,  Kirk R. Gustafson ,  Nancy H. Colburn ,  Matthew R. Young ,  James B. McMahon

Inventor： Curtis J. Henrich ,  Moon-Il Kang ,  Heidi R. Bokesch ,  Kirk R. Gustafson ,  Nancy H. Colburn ,  Matthew R. Young ,  James B. McMahon

IPC: A61K31/655 ,  A61P35/00 ,  A61P3/10 ,  A61P35/02 ,  A61P29/00 ,  A61P13/08 ,  A61P1/18 ,  A61P1/04 ,  A61P11/06 ,  C12Q1/02

CPC classification number: C07C309/66 ,  A61K31/10 ,  A61K31/635 ,  A61K31/655 ,  C07C317/32 ,  A61K2300/00

Abstract: An embodiment of the invention provides a pharmaceutical composition comprising a compound of formula (I)a pharmaceutically acceptable salt, prodrug, hydrate, or solvate thereof. Another embodiment of the invention provides a method of treating or preventing a condition associated with increased expression and/or activity of an NFκB pathway using same compounds. A further embodiment of the invention provides a method of diagnosing a condition in an individual using same compounds.

Abstract translation: 本发明的一个实施方案提供了包含式（I）化合物的药学组合物，其药学上可接受的盐，前药，水合物或溶剂合物。 本发明的另一个实施方案提供了使用相同化合物治疗或预防与增加NFκB途径的表达和/或活性相关的病症的方法。 本发明的另一个实施方案提供了使用相同化合物诊断个体状况的方法。

公开(公告)号：US07790764B2

公开(公告)日：2010-09-07

申请号：US11435189

申请日：2006-05-16

Applicant: Michael R Boyd ,  Kirk R Gustafson ,  Charles L Cantrell

Inventor： Michael R Boyd ,  Kirk R Gustafson ,  Charles L Cantrell

IPC: A01N43/02 ,  A61K31/335 ,  C07D309/00

CPC classification number: A61K31/395 ,  A61K31/365 ,  A61K31/7048 ,  C07D498/06 ,  C07D498/08

Abstract: The present invention provides a compound of formula (II).The present invention further provides a composition comprising at least one compound of the present invention and a pharmaceutically acceptable carrier, alone or in combination with at least one additional active agent. The present invention further provides a method of treating a condition treatable by the inhibition of vacuolar-type (H+)-ATPase and a method of treating cancer.

Abstract translation: 本发明提供式（II）化合物。 本发明还提供包含至少一种本发明化合物和药学上可接受的载体的组合物，其单独或与至少一种另外的活性剂组合。 本发明还提供了通过抑制液泡型（H +）-ATP酶处理可治疗的病症的方法和治疗癌症的方法。

公开(公告)号：US07144918B2

公开(公告)日：2006-12-05

申请号：US10333710

申请日：2001-07-24

Applicant: Michael R. Boyd ,  Kirk R. Gustafson ,  Charles L. Cantrell

Inventor： Michael R. Boyd ,  Kirk R. Gustafson ,  Charles L. Cantrell

IPC: A01N43/02 ,  A61K31/335 ,  C07D309/00

CPC classification number: A61K31/395 ,  A61K31/365 ,  A61K31/7048 ,  C07D498/06 ,  C07D498/08

Abstract: The present invention provides a compound of the formula (I).The present invention further provides a composition comprising at least one compound of the present invention and a pharmaceutically acceptable carrier, alone or in combination with at least one additional active agent. The present invention further provides a method of treating a condition treatable by the inhibition of vacuolar-type (H+)-ATPase and a method of treating cancer.

Abstract translation: 本发明提供式（I）的化合物。 本发明还提供包含至少一种本发明化合物和药学上可接受的载体的组合物，其单独或与至少一种另外的活性剂组合。 本发明还提供了通过抑制液泡型（H +）-ATP酶处理可治疗的病症的方法和治疗癌症的方法。

公开(公告)号：US5859049A

公开(公告)日：1999-01-12

申请号：US653006

申请日：1996-05-24

Applicant: Michael R. Boyd ,  John H. Cardellina, II ,  Kirk R. Gustafson ,  James B. McMahon ,  Richard W. Fuller ,  Gordon M. Cragg ,  Yoel Kashman ,  Doel Soejarto

Inventor： Michael R. Boyd ,  John H. Cardellina, II ,  Kirk R. Gustafson ,  James B. McMahon ,  Richard W. Fuller ,  Gordon M. Cragg ,  Yoel Kashman ,  Doel Soejarto

IPC: A61K31/365 ,  A61K31/366 ,  A61K36/18 ,  A61K45/06 ,  A61P31/12 ,  A61P31/18 ,  C07D493/14 ,  C07D493/22 ,  A61K31/37

CPC classification number: C07D493/14 ,  C07D493/22

Abstract: The present invention provides novel antiviral compounds, refered to as calanolides, related compounds, and their derivatives, which may be isolated from plants, or derived from compounds from plants, of the genus Calophyllum in accordance with the present inventive method. The compounds and their derivatives may be used alone or in combination with other antiviral agents in compositions, such as pharmaceutical compositions, to inhibit the growth or replication of a virus, such as a retrovirus, in particular a human immunodeficiency virus, specifically HIV-1 or HIV-2.

公开(公告)号：US5783598A

公开(公告)日：1998-07-21

申请号：US613162

申请日：1996-03-08

Applicant: Michael R. Boyd ,  John H. Cardellina, II ,  Kirk R. Gustafson ,  Laurent A. Decosterd ,  Ian Parson ,  Lewis Pannell ,  James B. McMahon ,  Gordon M. Cragg

Inventor： Michael R. Boyd ,  John H. Cardellina, II ,  Kirk R. Gustafson ,  Laurent A. Decosterd ,  Ian Parson ,  Lewis Pannell ,  James B. McMahon ,  Gordon M. Cragg

IPC: C07D211/46 ,  A61K31/00 ,  A61K31/12 ,  A61K31/35 ,  A61K31/352 ,  A61K31/37 ,  A61K31/505 ,  A61K31/52 ,  A61K31/70 ,  A61K38/00 ,  A61K38/17 ,  A61K38/21 ,  A61K45/06 ,  A61P31/00 ,  A61P31/12 ,  A61P31/18 ,  C07C46/00 ,  C07C46/10 ,  C07C50/32 ,  C07D311/46 ,  C07D311/54 ,  C07D311/56 ,  C07D311/92 ,  C07D407/14

CPC classification number: C07D311/92 ,  A61K31/12 ,  A61K31/35 ,  A61K31/352 ,  A61K31/37 ,  A61K31/70 ,  A61K38/1774 ,  A61K38/212 ,  A61K45/06 ,  C07C46/00 ,  C07C46/10 ,  C07C50/32 ,  C07D311/56

Abstract: The present invention provides novel antiviral naphthoquinone compounds, which may be isolated from plants of the genus Conospermum or synthesized chemically, in accordance with the present inventive methods. The antiviral naphthoquionone compounds, derivatives thereof, and prodrugs thereof, may be used alone or in combination with other antiviral agents in compositions, such as pharmaceutical compositions, to inhibit the growth or replication of a virus, such as a retrovirus, in particular a human immunodeficiency virus, specifically HIV-1 or HIV-2, in the treatment or prevention of viral infection.

Abstract translation: 本发明提供了新的抗病毒萘醌化合物，其可以根据本发明的方法从科氏菌属植物中分离或者化学合成。 抗病毒萘醌酮化合物，其衍生物及其前药可以单独使用或与组合物如药物组合物中的其它抗病毒剂组合使用，以抑制病毒如逆转录病毒，特别是人的生长或复制 免疫缺陷病毒，特别是HIV-1或HIV-2，用于治疗或预防病毒感染。