公开(公告)号：US20120277217A1

公开(公告)日：2012-11-01

申请号：US13501633

申请日：2010-10-27

申请人： Mario R. Mautino ,  Sanjeev Kumar ,  Firoz Jaipuri ,  Jesse Waldo ,  Tanay Kesharwani ,  Xiaoxia Zhang

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

IPC分类号： A61K31/4164 ,  C07D405/12 ,  A61K31/4178 ,  C07D403/12 ,  A61K31/497 ,  C07D409/12 ,  C07D401/12 ,  A61K31/4439 ,  A61K31/506 ,  A61K31/55 ,  C07D413/12 ,  A61K31/5377 ,  A61K31/496 ,  A61K31/454 ,  C07D487/04 ,  A61K31/4188 ,  A61P37/00 ,  C07D233/64

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。

公开(公告)号：US20110053941A1

公开(公告)日：2011-03-03

申请号：US12744860

申请日：2008-12-01

申请人： Mario Mautino ,  Firoz Jaipuri ,  Agnieszka Marcinowicz-Flick ,  Tanay Kesharwani ,  Jesse Waldo ,  Steven James Collier

发明人： Mario Mautino ,  Firoz Jaipuri ,  Agnieszka Marcinowicz-Flick ,  Tanay Kesharwani ,  Jesse Waldo ,  Steven James Collier

IPC分类号： A61K31/5375 ,  A61P37/00 ,  A61K31/135 ,  C07D209/14 ,  A61K31/4045 ,  A61K31/404 ,  C07D403/12 ,  C07D401/12 ,  A61K31/4709 ,  C07D405/12 ,  C07D413/12 ,  A61K31/423 ,  C07C333/04 ,  A61K31/27 ,  C07D213/53 ,  A61K31/4406 ,  A61K31/4402 ,  A61K31/36 ,  A61K31/381 ,  A61K31/47 ,  A61K31/357 ,  A61K31/428 ,  A61K31/505

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 ,  Y02A50/409 ,  Y02A50/465

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; （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-双加氧酶抑制量的化合物，如本文所述方面之一所述。

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：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：US20190225618A1

公开(公告)日：2019-07-25

申请号：US16269681

申请日：2019-02-07

申请人： Mario Mautino ,  Sanjeev Kumar ,  Jesse Waldo ,  Firoz Jaipuri ,  Tanay Kesharwani ,  Xiaoxia Zhang

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 immunosuppression associated with an infectious disease.

公开(公告)号：US10047066B2

公开(公告)日：2018-08-14

申请号：US12744860

申请日：2008-12-01

申请人： Mario Mautino ,  Firoz Jaipuri ,  Agnieszka Marcinowicz-Flick ,  Tanay Kesharwani ,  Jesse Waldo

发明人： Mario Mautino ,  Firoz Jaipuri ,  Agnieszka Marcinowicz-Flick ,  Tanay Kesharwani ,  Jesse Waldo

IPC分类号： A61K31/5375 ,  A61K31/135 ,  A61K31/404 ,  A61K31/381 ,  A61K31/505 ,  C07D209/14 ,  C07D405/12 ,  C07D333/56 ,  A61K31/138 ,  A61K31/506 ,  C07C259/06 ,  C07C311/48 ,  C07C327/44 ,  C07C327/48 ,  C07C333/20 ,  C07D209/18 ,  C07D213/40 ,  C07D215/26 ,  C07D253/07 ,  C07D261/20 ,  C07D263/22 ,  C07D277/36 ,  C07D279/06 ,  C07D307/81 ,  C07D333/58 ,  C07D333/60 ,  C07D335/06 ,  C07D401/06 ,  C07D409/12 ,  C07D417/06 ,  C07D417/12 ,  C07D277/64 ,  C07D307/80 ,  A61P37/00 ,  A61K31/4045 ,  C07D403/12 ,  C07D401/12 ,  A61K31/4709 ,  C07D413/12 ,  A61K31/423 ,  C07C333/04 ,  A61K31/27 ,  C07D213/53 ,  A61K31/4406 ,  A61K31/4402 ,  A61K31/36 ,  A61K31/47 ,  A61K31/357 ,  A61K31/428

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 ,  Y02A50/409 ,  Y02A50/465

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.

公开(公告)号：US08722720B2

公开(公告)日：2014-05-13

申请号：US13501633

申请日：2010-10-27

申请人： Mario R. Mautino ,  Sanjeev Kumar ,  Firoz Jaipuri ,  Jesse Waldo ,  Tanay Kesharwani

发明人： Mario R. Mautino ,  Sanjeev Kumar ,  Firoz Jaipuri ,  Jesse Waldo ,  Tanay Kesharwani

IPC分类号： A61K31/4174 ,  C07D233/64

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。