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1. 发明申请

WO2009132238A3 IDO INHIBITORS 审中-公开
标题翻译： IDO抑制剂
公开(公告)号：WO2009132238A3
公开(公告)日：2011-02-03
申请号：PCT/US2009041609
申请日：2009-04-24
申请人： NEWLINK GENETICS , LANKEANAU INST FOR MEDICAL RES , MAUTINO MARIO R , KUMAR SANJEEV , JAIPURI FIROZ , WALDO JESSE , KESHARWANI TANAY , VAHANIAN NICHOLAS N , LINK CHARLES J , LALONDE JUDITH , PRENDERGAST GEORGE , MULLER ALEXANDER , MALACHOWSKI WILLIAM
发明人： MAUTINO MARIO R , KUMAR SANJEEV , JAIPURI FIROZ , WALDO JESSE , KESHARWANI TANAY , VAHANIAN NICHOLAS N , LINK CHARLES J , LALONDE JUDITH , PRENDERGAST GEORGE , MULLER ALEXANDER , MALACHOWSKI WILLIAM
IPC分类号： A61K31/33 , A61P35/00
CPC分类号： C07D233/64 , A61K31/4174 , C07D233/56 , C07D233/58 , C07D233/60 , C07D233/61 , C07D401/12 , C07D403/12 , C07D413/12 , C07D417/06 , C07D498/04 , C07H19/067
摘要： Presently provided are compounds according to the formula (I) or (II), and pharmaceutical compositions comprising the compounds, wherein R1, R4, and R5 are defined herein. Such compounds and compositions are useful for modulating an activity of indoleamine 2,3-dioxygenase; treating indoleamine 2,3-dioxygenase (IDO) mediated immunosuppression; treating a medical conditions that benefit from the inhibition of enzymatic activity of indoleamine -2,3-dioxygenase; enhancing the effectiveness of an anti- cancer treatment comprising administering an anti-cancer agent; treating tumor-specific immunosuppression associated with cancer; and treating immunosupression associated with an infectious disease.
摘要翻译：目前提供的是根据式（I）或（II）的化合物和包含化合物的药物组合物，其中R1，R4和R5如本文所定义。这些化合物和组合物可用于调节吲哚胺2,3-双加氧酶的活性; 治疗吲哚胺2,3-双加氧酶（IDO）介导的免疫抑制; 治疗受抑制吲哚胺-2,3-双加氧酶的酶活性的医学病症; 提高抗癌治疗的有效性，包括施用抗癌剂; 治疗与癌症相关的肿瘤特异性免疫抑制; 并治疗与感染性疾病相关的免疫抑制。

2. 发明申请

WO2009073620A9 IDO INHIBITORS 审中-公开
公开(公告)号：WO2009073620A9
公开(公告)日：2009-06-11
申请号：PCT/US2008/085167
申请日：2008-12-01
申请人： NEWLINK GENETICS , MAUTINO, Mario , JAIPURI, Firoz , MARCINOWICZ-FLICK, Agnieszka , KESHARWANI, Tanay , WALDO, Jesse , COLLIER, Steven James
发明人： MAUTINO, Mario , JAIPURI, Firoz , MARCINOWICZ-FLICK, Agnieszka , KESHARWANI, Tanay , WALDO, Jesse , COLLIER, Steven James
IPC分类号： A61K31/506 , A61K31/00 , A61P31/00 , A61P35/00

3. 发明申请

WO2008057235A9 ENHANCED IMMUNOGENICITY OF TUMOR ASSOCIATED ANTIGENS BY ADDITION OF ALPHAGAL EPITOPES 审中-公开
标题翻译：添加表位加强肿瘤相关抗原的免疫原性
公开(公告)号：WO2008057235A9
公开(公告)日：2008-09-18
申请号：PCT/US2007022604
申请日：2007-10-25
申请人： NEWLINK GENETICS , JAIPURI FIROZ , MAUTINO MARIO R , VAHANIAN NICHOLAS N , YOUNG WON-BIN , ROSSI GABRIELA , LINK CHARLES J JR
发明人： JAIPURI FIROZ , MAUTINO MARIO R , VAHANIAN NICHOLAS N , YOUNG WON-BIN , ROSSI GABRIELA , LINK CHARLES J JR
IPC分类号： A61K39/00 , C07K5/00 , C12N15/00
CPC分类号： C07H5/04 , A61K31/70 , A61K39/0011 , A61K39/39 , A61K2039/55511 , C07H15/00 , C07H15/04
摘要： The invention relates to methods and compositions for causing the selective targeting and killing of tumor cells. The present invention describes prophylactic or therapeutic cancer vaccines based on purified TAA proteins or TAA-derived synthetic peptides altered by chemical, enzymatic or chemo-enzymatic methods to introduce aGal epitopes or aGal glycomimetic epitopes, in order to allow for enhanced opsonization of the antigen by natural anti-aGal antibodies to stimulate TAA capture and presentation, thereby inducing a humoral and cellular immune response to the TAA expressed by a tumor. The animal's immune system thus is stimulated to produce tumor specific cytotoxic cells and antibodies which will attack and kill tumor cells present in the animal.
摘要翻译：本发明涉及用于引起肿瘤细胞的选择性靶向和杀伤的方法和组合物。本发明描述了基于纯化的TAA蛋白或TAA衍生的合成肽的预防或治疗性癌症疫苗，所述合成肽通过化学，酶促或化学 - 酶促方法改变以引入Gal表位或Gal糖模拟表位，以允许通过以下方式增强抗原的调理作用：天然抗αGal抗体以刺激TAA捕获和呈递，从而诱导对由肿瘤表达的TAA的体液和细胞免疫应答。因此刺激动物的免疫系统产生肿瘤特异性细胞毒性细胞和抗体，其将攻击和杀死动物中存在的肿瘤细胞。

4. 发明申请

WO2012142237A8 FUSED IMIDAZOLE DERIVATIVES USEFUL AS IDO INHIBITORS 审中-公开
标题翻译：熔化的咪唑衍生物可用作IDO抑制剂
公开(公告)号：WO2012142237A8
公开(公告)日：2012-11-22
申请号：PCT/US2012033245
申请日：2012-04-12
申请人： NEWLINK GENETICS CORP , MAUTINO MARIO , KUMAR SANJEEV , WALDO JESSE , JAIPURI FIROZ , KESHARWANI TANAY
发明人： MAUTINO MARIO , KUMAR SANJEEV , WALDO JESSE , JAIPURI FIROZ , KESHARWANI TANAY
IPC分类号： C07D487/04 , A61K31/4188 , A61P37/02
CPC分类号： C07D487/04 , C07F9/6561
摘要： Presently provided are IDO inhibitors and pharmaceutical compositions thereof, useful for modulating an activity of indoleamine 2,3-dioxygenase; treating indoleamine 2,3-dioxygenase (IDO) mediated inimunosuppression; treating a medical conditions that benefit from the inhibition of enzymatic activity of indoleamine-2,3-dioxygenase; enhancing the effectiveness of an anti-cancer treatment comprising administering an anti-cancer agent; treating tumor-specific immunosuppression associated with cancer; and treating immunosupression associated with an infectious disease.
摘要翻译：目前提供的是可用于调节吲哚胺2,3-双加氧酶活性的IDO抑制剂及其药物组合物; 治疗吲哚胺2,3-双加氧酶（IDO）介导的抑制作用; 治疗受抑制吲哚胺-2,3-双加氧酶酶活性的医学病症; 提高抗癌治疗的有效性，包括施用抗癌剂; 治疗与癌症有关的肿瘤特异性免疫抑制; 并治疗与感染性疾病相关的免疫抑制。

5. 发明申请

WO2011056652A1 IMIDAZOLE DERIVATIVES AS IDO INHIBITORS 审中-公开
标题翻译：咪唑衍生物作为IDO抑制剂
公开(公告)号：WO2011056652A1
公开(公告)日：2011-05-12
申请号：PCT/US2010/054289
申请日：2010-10-27
申请人： NEWLINK GENETICS , MAUTINO, Mario, R. , KUMAR, Sanjeev , JAIPURI, Firoz , WALDO, Jesse , KESHARWANI, Tanay , ZHANG, Xiaoxia
发明人： MAUTINO, Mario, R. , KUMAR, Sanjeev , JAIPURI, Firoz , WALDO, Jesse , KESHARWANI, Tanay , ZHANG, Xiaoxia
IPC分类号： C07D233/64 , C07D401/12 , C07D403/12 , C07D407/12 , C07D409/12 , C07D413/12 , C07D417/12 , A61K31/4164 , A61K31/4178 , A61P35/00 , A61P37/00 , A61P31/00
CPC分类号： C07D233/64 , C07D401/12 , C07D403/12 , C07D407/12 , C07D409/12 , C07D413/12 , C07D417/12
摘要： Presently provided are IDO inhibitors of general formulae (VII), (VIII) as shown below and pharmaceutical compositions thereof, useful for modulating an activity of indoleamine 2,3-dioxygenase; treating indoleamine 2,3-dioxygenase (IDO) mediated immunosuppression; treating a medical conditions that benefit from the inhibition of enzymatic activity of indoleamine-2,3-dioxygenase; enhancing the effectiveness of an anti-cancer treatment comprising administering an anti-cancer agent; treating tumor-specific immunosuppression associated with cancer; and treating immunosupression associated with an infectious disease.
摘要翻译：目前提供的如下所示的通式（VII），（VIII）的IDO抑制剂及其药物组合物，其可用于调节吲哚胺2,3-双加氧酶的活性; 治疗吲哚胺2,3-双加氧酶（IDO）介导的免疫抑制; 治疗受抑制吲哚胺-2,3-双加氧酶酶活性的医学病症; 提高抗癌治疗的有效性，包括施用抗癌剂; 治疗与癌症有关的肿瘤特异性免疫抑制; 并治疗与感染性疾病相关的免疫抑制。

6. 发明申请

WO2008057235A2 ENHANCED IMMUNOGENICITY OF TUMOR ASSOCIATED ANTIGENS BY ADDITION OF ALPHAGAL EPITOPES 审中-公开
公开(公告)号：WO2008057235A2
公开(公告)日：2008-05-15
申请号：PCT/US2007022604
申请日：2007-10-25
申请人： NEWLINK GENETICS , JAIPURI FIROZ , MAUTINO MARIO R , VAHANIAN NICHOLAS N , YOUNG WON-BIN , ROSSI GABRIELA , LINK CHARLES J JR
发明人： JAIPURI FIROZ , MAUTINO MARIO R , VAHANIAN NICHOLAS N , YOUNG WON-BIN , ROSSI GABRIELA , LINK CHARLES J JR
IPC分类号： A61K39/00
CPC分类号： C07H5/04 , A61K31/70 , A61K39/0011 , A61K39/39 , A61K2039/55511 , C07H15/00 , C07H15/04
摘要： The invention relates to methods and compositions for causing the selective targeting and killing of tumor cells. The present invention describes prophylactic or therapeutic cancer vaccines based on purified TAA proteins or TAA-derived synthetic peptides altered by chemical, enzymatic or chemo-enzymatic methods to introduce aGal epitopes or aGal glycomimetic epitopes, in order to allow for enhanced opsonization of the antigen by natural anti-aGal antibodies to stimulate TAA capture and presentation, thereby inducing a humoral and cellular immune response to the TAA expressed by a tumor. The animal's immune system thus is stimulated to produce tumor specific cytotoxic cells and antibodies which will attack and kill tumor cells present in the animal.

7. 发明申请

WO2019006047A1 TDO2 AND IDO1 INHIBITORS 审中-公开
公开(公告)号：WO2019006047A1
公开(公告)日：2019-01-03
申请号：PCT/US2018/039880
申请日：2018-06-28
申请人： GENENTECH, INC. , NEWLINK GENETICS CORPORATION , PEI, Zhonghua , PARR, Brendan , LIU, Wendy , PASTOR, Richard , GAZZARD, Lewis , JAIPURI, Firoz , KUMAR, Sanjeev , POTTURI, Hima , WU, Guosheng , LIN, Xingyu , CHU, Yanyan , YUEN, Po-wai
发明人： PEI, Zhonghua , PARR, Brendan , LIU, Wendy , PASTOR, Richard , GAZZARD, Lewis , JAIPURI, Firoz , KUMAR, Sanjeev , POTTURI, Hima , WU, Guosheng , LIN, Xingyu , CHU, Yanyan , YUEN, Po-wai
IPC分类号： C07D487/04 , A61K31/437 , A61P35/00
摘要： Presently provided are inhibitors of TD02 and IDOl and pharmaceutical compositions thereof, useful for modulating an activity of tryptophan 2,3 dioxygenase and indoleamine 2,3- dioxygenase 1; treating immunosuppression; treating a medical conditions that benefit from the inhibition of tryptophan degradation; enhancing the effectiveness of an anti-cancer treatment comprising administering an anti-cancer agent; and treating tumor-specific immunosuppression associated with cancer.

8. 发明申请

WO2012142237A1 FUSED IMIDAZOLE DERIVATIVES USEFUL AS IDO INHIBITORS 审中-公开
标题翻译：融合的咪唑衍生物可用作IDO抑制剂
公开(公告)号：WO2012142237A1
公开(公告)日：2012-10-18
申请号：PCT/US2012/033245
申请日：2012-04-12
申请人： NEWLINK GENETICKS CORPORATION , MAUTINO, Mario , KUMAR, Sanjeev , WALDO, Jesse , JAIPURI, Firoz , KESHARWANI, Tanay
发明人： MAUTINO, Mario , KUMAR, Sanjeev , WALDO, Jesse , JAIPURI, Firoz , KESHARWANI, Tanay
IPC分类号： C07D487/04 , A61K31/4188 , A61P37/02
CPC分类号： C07D487/04 , C07F9/6561
摘要： Presently provided are IDO inhibitors and pharmaceutical compositions thereof, useful for modulating an activity of indoleamine 2,3-dioxygenase; treating indoleamine 2,3-dioxygenase (IDO) mediated inimunosuppression; treating a medical conditions that benefit from the inhibition of enzymatic activity of indoleamine-2,3-dioxygenase; enhancing the effectiveness of an anti-cancer treatment comprising administering an anti-cancer agent; treating tumor-specific immunosuppression associated with cancer; and treating immunosupression associated with an infectious disease.
摘要翻译：目前提供的是IDO抑制剂及其药物组合物，其可用于调节吲哚胺2,3-双加氧酶的活性; 治疗吲哚胺2,3-双加氧酶（IDO）介导的免疫抑制; 治疗受益于抑制吲哚胺-2,3-双加氧酶的酶活性的医学病症; 增强抗癌治疗的有效性，所述抗癌治疗包括施用抗癌剂; 治疗与癌症相关的肿瘤特异性免疫抑制; 并治疗与传染病相关的免疫抑制。

9. 发明申请

WO2009132238A2 IDO INHIBITORS 审中-公开
标题翻译： IDO抑制剂
公开(公告)号：WO2009132238A2
公开(公告)日：2009-10-29
申请号：PCT/US2009/041609
申请日：2009-04-24
申请人： NEWLINK GENETICS , LANKEANAU INSTITUTE FOR MEDICAL RESEARCH , MAUTINO, Mario, R. , KUMAR, Sanjeev , JAIPURI, Firoz , WALDO, Jesse , KESHARWANI, Tanay , VAHANIAN, Nicholas, N. , LINK, Charles, J. , LALONDE, Judith , PRENDERGAST, George , MULLER, Alexander , MALACHOWSKI, William
发明人： MAUTINO, Mario, R. , KUMAR, Sanjeev , JAIPURI, Firoz , WALDO, Jesse , KESHARWANI, Tanay , VAHANIAN, Nicholas, N. , LINK, Charles, J. , LALONDE, Judith , PRENDERGAST, George , MULLER, Alexander , MALACHOWSKI, William
IPC分类号： A61K31/538 , A61K31/4164
CPC分类号： C07D233/64 , A61K31/4174 , C07D233/56 , C07D233/58 , C07D233/60 , C07D233/61 , C07D401/12 , C07D403/12 , C07D413/12 , C07D417/06 , C07D498/04 , C07H19/067 , Y02A50/409 , Y02A50/465
摘要： Presently provided are compounds according to the formula (I) or (II), and pharmaceutical compositions comprising the compounds, wherein R 1 , R 4 , and R 5 are defined herein. Such compounds and compositions are useful for modulating an activity of indoleamine 2,3-dioxygenase; treating indoleamine 2,3-dioxygenase (IDO) mediated immunosuppression; treating a medical conditions that benefit from the inhibition of enzymatic activity of indoleamine -2,3-dioxygenase; enhancing the effectiveness of an anti- cancer treatment comprising administering an anti-cancer agent; treating tumor-specific immunosuppression associated with cancer; and treating immunosupression associated with an infectious disease.
摘要翻译：目前提供的是根据式（I）或（II）的化合物，以及包含化合物的药物组合物，其中R 1，R 4和R 5在本文中定义。这些化合物和组合物可用于调节吲哚胺2,3-双加氧酶的活性; 治疗吲哚胺2,3-双加氧酶（IDO）介导的免疫抑制; 治疗受抑制吲哚胺-2,3-双加氧酶的酶活性的医学病症; 增强抗癌治疗的有效性，包括施用抗癌剂; 治疗与癌症有关的肿瘤特异性免疫抑制; 并治疗与感染性疾病相关的免疫抑制。

10. 发明申请

WO2009073620A2 IDO INHIBITORS 审中-公开
标题翻译： IDO抑制剂
公开(公告)号：WO2009073620A2
公开(公告)日：2009-06-11
申请号：PCT/US2008085167
申请日：2008-12-01
申请人： NEWLINK GENETICS , MAUTINO MARIO , JAIPURI FIROZ , MARCINOWICZ-FLICK AGNIESZKA , KESHARWANI TANAY , WALDO JESSE
发明人： MAUTINO MARIO , JAIPURI FIROZ , MARCINOWICZ-FLICK AGNIESZKA , KESHARWANI TANAY , WALDO JESSE
IPC分类号： A61K31/506
CPC分类号： C07D333/56 , A61K31/138 , A61K31/506 , C07C259/06 , C07C311/48 , C07C327/44 , C07C327/48 , C07C333/20 , C07D209/14 , C07D209/18 , C07D213/40 , C07D215/26 , C07D253/07 , C07D261/20 , C07D263/22 , C07D277/36 , C07D277/64 , C07D279/06 , C07D307/80 , C07D307/81 , C07D333/58 , C07D333/60 , C07D335/06 , C07D401/06 , C07D405/12 , C07D409/12 , C07D417/06 , C07D417/12
摘要： Presently provided are methods for (a) modulating an activity of indoleamine 2,3-dioxygenase comprising contacting an indoleamine 2,3-dioxygenase with a modulation effective amount of a compound as described in one of the aspects described herein; (b) treating indoleamine 2,3-dioxygenase (IDO) mediated immunosuppression in a subject in need thereof, comprising administering an effective indoleamine 2,3-dioxygenase inhibiting amount of a compound as described in one of the aspects described herein; (c) treating a medical conditions that benefit from the inhibition of enzymatic activity of indoleamine-2,3-dioxygenase comprising administering an effective indoleamine 2,3-dioxygenase inhibiting amount of a compound as described in one of the aspects described herein; (d) enhancing the effectiveness of an anti-cancer treatment comprising administering an anti-cancer agent and a compound as described in one of the aspects described herein; (e) treating tumor-specific immunosuppression associated with cancer comprising administering an effective indoleamine 2,3-dioxygenase inhibiting amount of a compound as described in one of the aspects described herein; and (f) treating immunosuppression associated with an infectious disease, e.g., HIV-I infection, comprising administering an effective indoleamine 2,3-dioxygenase inhibiting amount a compound as described in one of the aspects described herein.
摘要翻译：目前提供的是（a）调节吲哚胺2,3-双加氧酶的活性的方法，包括使吲哚胺2,3-双加氧酶与调节有效量的化合物的接触，如本文所述的一个方面所述; （b）在有需要的受试者中治疗吲哚胺2,3-双加氧酶（IDO）介导的免疫抑制，包括施用有效的吲哚胺2,3-双加氧酶抑制量的本文所述方面之一所述的化合物; （c）治疗受抑于吲哚胺-2,3-双加氧酶的酶活性的医学病症，包括给予有效的吲哚胺2,3-双加氧酶抑制量的本文所述方面之一所述的化合物; （d）增强抗癌治疗的有效性，包括给予本文所述方面之一所述的抗癌剂和化合物; （e）治疗与癌症相关的肿瘤特异性免疫抑制，包括施用有效的吲哚胺2,3-双加氧酶抑制量的本文所述方面之一所述的化合物; 和（f）治疗与感染性疾病例如HIV-1感染相关的免疫抑制，包括给予有效的吲哚胺2,3-双加氧酶抑制量的如本文所述方面之一所述的化合物。

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