公开(公告)号：US20040131629A1

公开(公告)日：2004-07-08

申请号：US10670797

申请日：2003-09-26

Applicant: Panacos Pharmaceuticals, Inc. ,  The University of North Carolina at Chapel Hill ,  Niigata University of Pharmacy and Applied Science

Inventor： Graham P. Allaway ,  Carl T. Wild ,  Yoshiki Kashiwada ,  Kuo-Hsiung Lee

IPC: A61K031/56 ,  A61K039/00 ,  C07J053/00

CPC classification number: C07J63/008 ,  A61K31/56 ,  A61K45/06 ,  C07J53/00 ,  A61K2300/00

Abstract: Betulin and dihydrobetulin acyl derivatives according to the present invention have been found to have potent anti-HIV activity. The compounds of the present invention have Formula I as described herein, or pharmaceutically acceptable salts thereof, wherein R1 is a C2-C20 substituted or unsubstituted carboxyacyl, R2 is hydrogen, chloro, bromo, or hydroxy, R4 is hydrogen or C(C6H5)3; wherein the dashed line represents an optional double bond between C20 and C29.

Abstract translation: 已经发现根据本发明的桦木醇和二氢甜菜碱酰基衍生物具有有效的抗HIV活性。 本发明化合物具有本文所述的式I或其药学上可接受的盐，其中R 1为C 2 -C 20取代或未取代的羧基酰基，R 2为氢，氯，溴或羟基，R 4为氢或C（C 6 H 5） 3; 其中虚线表示C20和C29之间任选的双键。

公开(公告)号：US20040213801A1

公开(公告)日：2004-10-28

申请号：US10660206

申请日：2003-09-10

Applicant: Panacos Pharmaceuticals, Inc.

Inventor： Carl T. Wild ,  Carol D. Weiss

IPC: A61K039/21 ,  C07K014/16

CPC classification number: C07K14/005 ,  A61K39/00 ,  A61K47/62 ,  A61K2039/505 ,  C07K16/1063 ,  C07K2317/34 ,  C12N2740/16122

Abstract: The present invention is directed to the induction and characterization of a humoral immune response targeting nullentry-relevantnull gp41 structures. In its broadest aspect, the present invention is directed to methods of raising a neutralizing antibody response to a broad spectrum of HIV strains and isolates. The present invention targets particular molecular conformations or structures that occur at the cell surface of HIV during viral entry into host cells. Such a humoral response can be generated in vivo as a prophylactic measure in individuals to reduce or inhibit the ability of HIV to infect uninfected cells in the individual's body. Such a response can also be employed to raise antibodies against nullentry relevantnull gp41 structures. These antibodies can be employed for therapeutic uses, and as tools for further illuminating the mechanism of HIV cell entry.

Abstract translation: 本发明涉及针对“入门相关”gp41结构的体液免疫应答的诱导和表征。 在其最广泛的方面，本发明涉及提高对广谱的HIV菌株和分离物的中和抗体应答的方法。 本发明针对在病毒进入宿主细胞期间发生在HIV细胞表面的特定分子构象或结构。 这样的体液应答可以在个体中作为预防措施在体内产生，以减少或抑制HIV感染个体身体中未感染细胞的能力。 也可以采用这种反应来产生针对“进入相关”gp41结构的抗体。 这些抗体可用于治疗用途，以及作为用于进一步照射HIV细胞进入机制的工具。

公开(公告)号：US20030008891A1

公开(公告)日：2003-01-09

申请号：US10096107

申请日：2002-03-13

Applicant: Panacos Pharmaceuticals, Inc.

Inventor： Kuo-Hsiung Lee ,  Lan Xie ,  Graham P. Allaway ,  Carl T. Wild

IPC: A61K031/4741 ,  C07D471/02 ,  C07D335/08 ,  C07D335/10

CPC classification number: C07D471/04 ,  C07D493/04 ,  C07D495/04 ,  C07F9/6561

Abstract: 3null,4null-di-O-camphanoyl-(null)-cis-khellactone analogs according to the present invention have been found to have anti-HIV activity. The compounds of the present invention have the following formula: 1 or a pharmaceutically acceptable salt, ester or prodrug thereof, wherein R1, R2, R3, R4, X, and Z are set in the specification. The invention is also directed to pharmaceuticals compositions comprising one or more compounds of Formula I, optionally further comprising one or more anti-viral agents or immunostimulating agents. Further, the invention is directed to the use of compounds of Formula I for the inhibition of a retroviral infection in cells or tissue of an animal, for the treatment of a patient suffering from a retroviral-related pathology, for the prevention of transmission of HIV infection from an HIV infected pregnant woman to a fetus, and for the prevention of transmission of HIV infection during sexual intercourse.

Abstract translation: 已经发现根据本发明的3'，4'-二-O-樟脑酰 - （+） - 顺 - 壳内酯类似物具有抗HIV活性。 本发明的化合物具有下式：或其药学上可接受的盐，酯或前药，其中R1，R2，R3，R4，X和Z置于说明书中。 本发明还涉及包含一种或多种式I化合物的药物组合物，任选地还包含一种或多种抗病毒剂或免疫刺激剂。 此外，本发明涉及式I化合物用于抑制动物细胞或组织中的逆转录病毒感染，用于治疗患有逆转录病毒相关病理学的患者，用于预防HIV传播 感染艾滋病毒的孕妇到胎儿的感染，以及在性交期间预防艾滋病毒感染的传播。

公开(公告)号：US20040132011A1

公开(公告)日：2004-07-08

申请号：US10685801

申请日：2003-10-16

Applicant: Panacos Pharmaceuticals, Inc.

Inventor： Graham P. Allaway ,  Carl T. Wild ,  Karl Salzwedel

IPC: C12Q001/70

CPC classification number: G01N33/56988 ,  C12Q1/703 ,  G01N33/5014

Abstract: The invention is directed to methods for identifying compounds that decrease the ability of a virus, such as HIV-1, to infect previously uninfected cells by inducing conformational changes in viral envelope proteins, and the compounds discovered by such methods.

Abstract translation: 本发明涉及鉴定通过诱导病毒包膜蛋白质构象变化和通过这些方法发现的化合物来鉴定降低病毒如HIV-1的病毒感染先前未感染细胞的化合物的方法。

公开(公告)号：TW200837074A

公开(公告)日：2008-09-16

申请号：TW096141450

申请日：2007-11-02

Applicant: 派那可斯製藥股份有限公司 PANACOS PHARMACEUTICALS, INC.

Inventor： 費爾朶 尼茲 NITZ, THEODORE JOHN ,  克利斯汀 蒙特貝堤 MONTALBETTI, CHRISTIAN ,  理查 米爾斯 MEARS, RICHARD ,  蓋新杰 GAI, XINJIE ,  艾德華 葛倫 GLENN, EDWARD

IPC: C07J

CPC classification number: C07J63/008 ,  A61K31/57 ,  A61K31/58 ,  A61K45/06 ,  C07J53/00

Abstract: 本發明係有關新穎之藥學活性的三烯衍生物、含彼之藥學組成物、其作為藥物之用途、及該化合物之用於製造特定藥物的用途。本發明亦有關一種包括投服該化合物之治療方法。詳言之,所述之化合物是在C-3、C2-8和C-19位置中之一或多者具有取代基之樺木酸(betulinic acid)的衍生物,如文中所述。此新穎化合物可用作為抗病毒劑。特別地,該新穎化合物可用於治療人類免疫缺陷病毒(HIV)。

Abstract in simplified Chinese: 本发明系有关新颖之药学活性的三烯衍生物、含彼之药学组成物、其作为药物之用途、及该化合物之用于制造特定药物的用途。本发明亦有关一种包括投服该化合物之治疗方法。详言之,所述之化合物是在C-3、C2-8和C-19位置中之一或多者具有取代基之桦木酸(betulinic acid)的衍生物,如文中所述。此新颖化合物可用作为抗病毒剂。特别地,该新颖化合物可用于治疗人类免疫缺陷病毒(HIV)。

公开(公告)号：TW200628161A

公开(公告)日：2006-08-16

申请号：TW094139647

申请日：2005-11-11

Applicant: 派那可斯製藥股份有限公司 PANACOS PHARMACEUTICALS, INC. ,  費爾朶 尼茲 NITZ, THOEDORE JOHN ,  蓋瑞 魯賓森 ROBINSON, GARY N. ,  卡爾 魏爾德 WILD, CARL T. ,  馬克 艾許頓 ASHTON, MARK ,  羅梭 湯瑪斯 THOMAS, RUSSELL ,  克利斯汀 蒙特貝堤 MONTALBETTI, CHRISTIAN ,  湯瑪斯 庫爾特 COULTER, THOMAS STEPHEN ,  菲利波 瑪嘉羅西 MAGARACI, FILIPPO ,  羅勃特 湯賽德 TOWNSEND, ROBERT JAMES

Inventor： 費爾朶 尼茲 NITZ, THOEDORE JOHN ,  蓋瑞 魯賓森 ROBINSON, GARY N. ,  卡爾 魏爾德 WILD, CARL T. ,  馬克 艾許頓 ASHTON, MARK ,  羅梭 湯瑪斯 THOMAS, RUSSELL ,  克利斯汀 蒙特貝堤 MONTALBETTI, CHRISTIAN ,  湯瑪斯 庫爾特 COULTER, THOMAS STEPHEN ,  菲利波 瑪嘉羅西 MAGARACI, FILIPPO ,  羅勃特 湯賽德 TOWNSEND, ROBERT JAMES

IPC: A61K ,  C07J

CPC classification number: C07J51/00 ,  C07J53/00

Abstract: 本發明係有關新穎之樺木醇的合成衍生物及該衍生物作為藥物之用途。本發明係有關如下式I所示之新穎化合物：094139647-p01.bmp或其藥學上可接受之鹽或前驅藥物。094139647-p01.bmp

Abstract in simplified Chinese: 本发明系有关新颖之桦木醇的合成衍生物及该衍生物作为药物之用途。本发明系有关如下式I所示之新颖化合物：094139647-p01.bmp或其药学上可接受之盐或前驱药物。094139647-p01.bmp

公开(公告)号：WO2009042166A1

公开(公告)日：2009-04-02

申请号：PCT/US2008/011094

申请日：2008-09-25

Applicant: PANACOS PHARMACEUTICALS, INC. ,  JACOB, Jules ,  RICHARDS, John ,  AUGUSTINE, John, G. ,  MILEA, Jaqueline, S.

Inventor： JACOB, Jules ,  RICHARDS, John ,  AUGUSTINE, John, G. ,  MILEA, Jaqueline, S.

IPC: A61K45/06

CPC classification number: A61K31/565 ,  A61K9/0095 ,  A61K9/14 ,  A61K47/34 ,  A61K47/40

Abstract: The present application discloses and claims liquid pharmaceutical compositions comprising bevirimat dimeglumine as a drug substance, methods of treatment comprising administering such compositions to a subject in need thereof, and the use of such compositions in the manufacture of medicaments.

Abstract translation: 本申请公开并要求含有作为药物物质的贝伐单抗二葡胺的液体药物组合物，治疗方法包括向有需要的受试者施用此类组合物，以及这些组合物在制备药物中的用途。

公开(公告)号：WO2008134035A1

公开(公告)日：2008-11-06

申请号：PCT/US2008/005428

申请日：2008-04-28

Applicant: PANACOS PHARMACEUTICALS, INC. ,  NITZ, Theodore, J. ,  SALZWEDEL, Karl ,  FINNEGAN, Catherine ,  WILD, Carl ,  BRUNTON, Shirley ,  FLANAGAN, Stuart ,  MONTALBETTI, Christian ,  COULTER, Thomas, Stephen ,  KIMBER, Marc ,  MAGARACI, Filippo ,  JOHNSTON, David

Inventor： NITZ, Theodore, J. ,  SALZWEDEL, Karl ,  FINNEGAN, Catherine ,  WILD, Carl ,  BRUNTON, Shirley ,  FLANAGAN, Stuart ,  MONTALBETTI, Christian ,  COULTER, Thomas, Stephen ,  KIMBER, Marc ,  MAGARACI, Filippo ,  JOHNSTON, David

IPC: C07D487/04 ,  A61P31/12 ,  A61K31/519

CPC classification number: C07D487/04

Abstract: Methods of preventing, treating or delaying the onset of HIV in a subject by administering to the subject novel pharmaceutically active arylmethyl pyrazolo[1,5-α ]pyrimidine amide derivatives, or pharmaceutical compositions containing the same are described. Additionally, compounds of novel pharmaceutically active arylmethyl piperazine pyrazolo[l,5-α]pyrimidine amide derivatives and their use for the manufacture of specific medicaments are described.

Abstract translation: 描述了通过向受试者施用药学活性的芳基甲基吡唑并[1,5-a]嘧啶酰胺衍生物或含有它们的药物组合物来预防，治疗或延迟受试者中HIV发病的方法。 此外，描述了新的药学活性的芳基甲基哌嗪吡唑并[1,5-a]嘧啶酰胺衍生物的化合物及其制备特定药物的用途。

公开(公告)号：WO2004069166A3

公开(公告)日：2004-08-19

申请号：PCT/US2004/002393

申请日：2004-01-29

Applicant: PANACOS PHARMACEUTICALS, INC. ,  THE GOVERNMENT OF THE UNITED STATES OF AMERICA, as represented by the Secretary, DEPARTMENT OF HEALTH AND HUMAN SERVICES ,  SALZWEDEL, Karl ,  LI, Feng ,  WILD, Carl, T. ,  ALLAWAY, Graham, P. ,  FREED, Eric, O.

Inventor： SALZWEDEL, Karl ,  LI, Feng ,  WILD, Carl, T. ,  ALLAWAY, Graham, P. ,  FREED, Eric, O.

IPC: A01N37/02

Abstract: Inhibition of HIV-1 replication by disrupting the processing of the viral Gag capsid (CA) protein (p24) from the CA-spacer peptide 1 (SP1) protein precursor (p25) is disclosed. Amino acid sequences containing a mutation in the Gag p25 protein, with the mutation resulting in a decrease in the inhibition of processing of p25 to p24 by dimethylsuccinyl betulinic acid or dimethylsuccinyl betulin, polynucleotides encoding such mutated sequences and antibodies that selectively bind such mutated sequences are also included. Methods of inhibiting, inhibitory compounds and methods of discovering inhibitory compounds that target proteolytic processing of the HIV Gag protein are included. In one embodiment, such compounds inhibit the interaction of the HIV protease enzyme with Gag by binding to the Gag proteolytic cleavage site rather than to the protease enzyme. In another embodiment, viruses or recombinant proteins that contain mutations in the region of the Gag proteolytic cleavage site can be used in screening assays to identify compounds that target proteolytic processing.

公开(公告)号：WO2004035808A2

公开(公告)日：2004-04-29

申请号：PCT/US0332582

申请日：2003-10-16

Applicant: PANACOS PHARMACEUTICALS INC ,  ALLAWAY GRAHAM P ,  WILD CARL T ,  SALZWEDEL KARL

Inventor： ALLAWAY GRAHAM P ,  WILD CARL T ,  SALZWEDEL KARL

IPC: C12Q1/70 ,  G01N33/50 ,  G01N33/569 ,  C12Q

CPC classification number: G01N33/56988 ,  C12Q1/703 ,  G01N33/5014

Abstract: The invention is directed to methods for identifying compounds that decrease the ability of a virus, such as HIV-1, to infect previously uninfected cells by inducing conformational changes in viral envelope proteins, and the compounds discovered by such methods.