公开(公告)号：US20240132507A1

公开(公告)日：2024-04-25

申请号：US18496146

申请日：2023-10-27

申请人： Genentech, Inc. ,  NewLink Genetics Corporation

发明人： Zhonghua Pei ,  Brendan Parr ,  Wendy Liu ,  Richard Pastor ,  Lewis Gazzard ,  Firoz Jaipuri ,  Sanjeev Kumar ,  Hima Potturi ,  Guoshen Wu ,  Xingyu Lin ,  Yanyan Chu ,  Po-wai Yuen

IPC分类号： C07D487/04

CPC分类号： C07D487/04

摘要： Presently provided are inhibitors of TD02 and IDO1 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.

公开(公告)号：US09981973B2

公开(公告)日：2018-05-29

申请号：US15434414

申请日：2017-02-16

申请人： NewLink Genetics Corporation

发明人： Sanjeev Kumar ,  Jesse Waldo ,  Firoz Jaipuri ,  Mario Mautino

IPC分类号： C07D235/02 ,  C07D487/04

CPC分类号： C07D487/04 ,  C07D235/02

摘要： Presently provided are inhibitors of IDO and TDO and pharmaceutical compositions thereof, useful for modulating an activity of indoleamine 2,3-dioxygenase and tryptophan 2,3 dioxygenase; 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; treating tumor-specific immunosuppression associated with cancer; and treating immunosuppression associated with an infectious disease.

公开(公告)号：US09512158B2

公开(公告)日：2016-12-06

申请号：US13716570

申请日：2012-12-17

申请人： NewLink Genetics Corp.

发明人： Mario R. Mautino ,  Nicholas N. Vahanian ,  Won-Bin Young ,  Gabriela Rossi ,  Charles J. Link ,  Firoz Jaipuri

IPC分类号： A61K39/00 ,  C07H5/04 ,  C07H15/04 ,  C07H15/00 ,  A61K39/39 ,  A61K31/70

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 αGal epitopes or αGal glycomimetic epitopes, in order to allow for enhanced opsonization of the antigen by natural anti-αGal 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.

公开(公告)号：US08748469B2

公开(公告)日：2014-06-10

申请号：US12988391

申请日：2009-04-24

申请人： Mario R. Mautino ,  Sanjeev Kumar ,  Firoz Jaipuri ,  Jesse Waldo ,  Tanay Kesharwani ,  Nicholas N. Vahanian ,  Charles J. Link

发明人： Mario R. Mautino ,  Sanjeev Kumar ,  Firoz Jaipuri ,  Jesse Waldo ,  Tanay Kesharwani ,  Nicholas N. Vahanian ,  Charles J. Link

IPC分类号： A61K31/4174

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 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，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; 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。

公开(公告)号：US20130178613A1

公开(公告)日：2013-07-11

申请号：US13716569

申请日：2012-12-17

申请人： NewLink Genetics Corp.

发明人： Mario R. MAUTINO ,  Nicholas N. Vahanian ,  Won-Bin Young ,  Gabriela Rossi ,  Charles J. Link ,  Firoz Jaipuri

IPC分类号： C07H5/04

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 αGal epitopes or αGal glycomimetic epitopes, in order to allow for enhanced opsonization of the antigen by natural anti-αGal 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.

公开(公告)号：US20110136796A1

公开(公告)日：2011-06-09

申请号：US12988391

申请日：2009-04-24

申请人： Mario R. Mautino ,  Sanjeev Kumar ,  Firoz Jaipuri ,  Jesse Waldo ,  Tanay Kesharwani ,  Nicholas N. Vahanian ,  Charles J. Link ,  Judith Lalonde ,  George Prendergast ,  Alexander Muller ,  William Malachowski

发明人： Mario R. Mautino ,  Sanjeev Kumar ,  Firoz Jaipuri ,  Jesse Waldo ,  Tanay Kesharwani ,  Nicholas N. Vahanian ,  Charles J. Link ,  Judith Lalonde ,  George Prendergast ,  Alexander Muller ,  William Malachowski

IPC分类号： A61K31/541 ,  C07D233/56 ,  C07D417/06 ,  C07D319/08 ,  C07D401/12 ,  C07D413/12 ,  A61K31/4164 ,  A61K31/357 ,  A61K31/454 ,  A61K31/5377 ,  A61K31/506 ,  A61P37/04 ,  A61P31/04 ,  A61P35/00 ,  A61P35/02

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 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，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; 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。

公开(公告)号：US10800780B2

公开(公告)日：2020-10-13

申请号：US16065397

申请日：2016-12-23

申请人： Genentech, Inc. ,  NewLink Genetics Corporation

发明人： Xingyu Lin ,  Po-wai Yuen ,  Rohan Mendonca ,  Brendan Parr ,  Richard Pastor ,  Zhonghua Pei ,  Lewis Gazzard ,  Firoz Jaipuri ,  Sanjeev Kumar ,  Xiaokai Li ,  Roheeth Pavana ,  Hima Potturi ,  Venkata Velvadapu ,  Jesse Waldo ,  Zuhui Zhang ,  Guosheng Wu ,  Benjamin Douglas Sellers

IPC分类号： A61K31/4188 ,  A61K31/407 ,  A61K31/4035 ,  C07D487/04 ,  C07D519/00 ,  A61P35/00 ,  A61K45/06 ,  A61K38/16

摘要： Presently provided are inhibitors of cellularly expressed TDO2 and pharmaceutical compositions thereof, useful for modulating an activity of tryptophan 2, 3 dioxygenase; 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.

公开(公告)号：US10233190B2

公开(公告)日：2019-03-19

申请号：US15800190

申请日：2017-11-01

申请人： NewLink Genetics Corporation

发明人： Mario Mautino ,  Sanjeev Kumar ,  Jesse Waldo ,  Firoz Jaipuri ,  Tanay Kesharwani ,  Xiaoxia Zhang

IPC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 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.

公开(公告)号：US09732035B2

公开(公告)日：2017-08-15

申请号：US15171031

申请日：2016-06-02

申请人： NewLink Genetics, Corp.

发明人： Mario Mautino ,  Sanjeev Kumar ,  Firoz Jaipuri ,  Jesse Waldo ,  Hima Potturi ,  Hong Zhuang

IPC分类号： A61K31/675 ,  A61K31/405 ,  C07F9/02 ,  C07D209/20 ,  C07F9/6574 ,  C07D405/12 ,  C07D401/12 ,  C07C309/04 ,  C07C309/20

CPC分类号： C07D209/20 ,  A61K31/285 ,  C07C309/04 ,  C07C309/20 ,  C07D401/12 ,  C07D405/12 ,  C07F9/65742

摘要： Presently provided are indoximod prodrug and salt compounds and pharmaceutical compositions comprising salts and prodrugs of indoximod, that produce enhanced plasma concentration and exposure to indoximod compared to direct administration of indoximod, in patients in need of treatment of immunosuppression mediated by the indoleamine-2,3-dioxygenase pathway, such as patients with cancer or chronic infectious diseases.

公开(公告)号：US20140323740A1

公开(公告)日：2014-10-30

申请号：US14264974

申请日：2014-04-29

申请人： NewLink Genetics Corporation ,  Lankeanau Institute for Medical Research

发明人： Mario R. Mautino ,  Sanjeev Kumar ,  Firoz Jaipuri ,  Jesse Waldo ,  Tanay Kesharwani ,  Nicholas N. Vahanian ,  Charles J. Link ,  Judith Lalonde ,  George Prendergast ,  Alexander Muller ,  William Malachowski

IPC分类号： C07D233/64

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 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，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; 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。